CHEMDNER_TEST_TEXT/ 0000755 0023442 0023420 00000000000 12563124501 015267 5 ustar mkrallinger BioinfoUnix CHEMDNER_TEST_TEXT/chemdner_patents_test_background_text_release.txt 0000640 0023442 0023420 00147474754 12563116050 027412 0 ustar mkrallinger BioinfoUnix CN102961377A Method for preparing compound amino acid injection liquid (20AA) The invention mainly relates to a method for preparing compound amino acid injection liquid (20AA), and belongs to the technical field of medicines. The problems that the amino acid is oxidized and degraded and solution color is deepened because the solution is in contact with oxygen for a long time during preparation and filling are solved by vacuumizing and filling nitrogen during preparation of the injection liquid. In the method, the injection liquid is dissolved in batch or in several times according to the dissolution difficulty of amino acid, so that the problem that the indissolvable amino acid crystal separates out during preparation is solved, and the stability and the quality of the amino acid injection liquid are guaranteed to the maximum limit. The method has the advantages of simple operation, scientific and reasonable process, low cost and low requirement on production equipment.
EP1673985A1 Functional sweetener The present invention provides a sweetener wherein corosolic acid, and at least one selected from the group consisiting of a sucrase inhibitor and indigestible dextrin, are added to sucrose.
US6914046 Administering human growth hormone having a specific amino acid sequence to cancer patients who are resistant to, or at risk of developing a resistance to a NF-kappa B-activating cytotoxic molecule Compounds inhibiting the activation of the nuclear factor κB (NF-κB) are used for the preparation of medications adapted for the treatment of malignant hemopathies and solid tumors, and for the prevention of the appearance or the treatment, of phenomena of resistance to cytotoxic molecules used in the scope of treatment of the above pathologies, appearing in patients treated with these molecules when the latter are adapted to activate NF-κB.
WO2014092061A1 Hydantoin derivative The present invention consists of a compound that can be represented by general formula (1) or a pharmacologically permitted salt thereof. (1) (In the formula, R1, R2, R3, and R4 are as defined in the claims.)
WO2010061862A1 Antitumor agent containing thalidomide derivative as active ingredient Disclosed is an antitumor agent which contains, as an active ingredient, a thalidomide derivative selected from the compounds shown below.
WO2013079668A1 Piperidine derivatives, pharmaceutical compositions and uses thereof The invention relates to new piperidine derivatives of the formula (I) to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
EP1698332A1 Oral modified release formulations containing 8-Prenylnaringenin for continuous estrogen support This invention is directed to an oral modified release formulation of the phytoestrogen 8-Prenylnaringenin and its use for the treatment of symptoms of estrogen deficiency.
US20060270689 Novel Fused Heterocycles and Uses Thereof This invention relates to novel compounds having the formula (I) (a chemical formula should be inserted here—please see paper copy enclosed herewith) m=0, 1, 2 n=0, 1 (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
WO2012015168A2 Pharmaceutical composition comprising rosuvastatin or a pharmaceutically acceptable salt thereof Provided is a pharmaceutical composition comprising rosuvastatin or a pharmaceutically acceptable salt thereof and an anhydrous dibasic calcium phosphate as a stabilizer. The composition of the present invention has outstanding storage stability.
CN102600201A Pharmaceutical composition for relaxing bowels and purging intestines and preparation method of pharmaceutical composition The invention provides a pharmaceutical composition for relaxing bowels and purging intestines, wherein the pharmaceutical composition comprises polyethylene glycol with a molecular weight distribution of 3,300-3,800. As polyethylene glycol with the molecular weight distribution of 3,300-3,800 is contained, the pharmaceutical composition for relaxing bowels and purging intestines provided by the invention not only has better effects of relaxing bowels and purging intestines than those of the existing medicines containing polyethylene glycol with a molecular weight of 4,000 and polyethylene glycol with a molecular weight of 3,350, but also has the advantages of good taste and few side effects of bowels relaxing and intestines purging, so that the pharmaceutical composition is more helpful for the clinical treatment of the constipation and the preparation of cleaning the intestines before an operation. The invention also provides a preparation method of the pharmaceutical composition. By adopting the preparation method, the molecular weight distribution of polyethylene glycol which is the major ingredient of the pharmaceutical composition can be accurately controlled in a range of 3,300-3,800.
CN1895672A Multifunctional broad-spectrum obtundent of polyphyletic synergistic and its use A multi-element synergistic disinfecting analgetic with multiple functions and broad spectrum contains matrix, antibacterial antalgic compound, antimicrobial compound, quaternary ammonium salt compound, and/or chlorophenol compound. Its application is also disclosed.
CN102442964A N1, N4-di-n-butyl-3, 6-dimethyl-1, 2, 4, 5-tetrazine-1, 4-dicarboximide as well as preparation method and application thereof The invention discloses an N1, N4-di-n-butyl-3, 6-dimethyl-1, 2, 4, 5-tetrazine-1, 4-dicarboximide compound shown as a formula (I) as well as a preparation method and a purpose thereof. The compound is prepared by using 3, 6-dimethyl-1, 6-dihydro-1, 2, 4, 5-tetrazine and triphosgene (BTC) as raw materials to take reaction with n-butylamine in organic solvents under the effect of base catalysis. The compound is applied to the preparation of medicine for treating and preventing human gastric cancer and human ovarian cancer diseases. The compound as well as the preparation method and the purpose have the advantages that the design is reasonable, the preparation method is simple and convenient, the operation is easy, the raw materials are easy to obtain, in addition, the production cost is low, the compound is suitable for industrial application, and a new variety is provided for the anti-tumor medicine screening.
CN101497623B Compound containing imidazopyridine The invention belongs to the technical field of medicine, and in particular relates to compounds which are shown in a general formula (I) and contain imidazopyridine, pharmaceutically acceptable salts of the same and isomers of the same, wherein R<1>, R<2>, R<3>, and X are defined in a specification. The invention also relates to a method for preparing the compounds, a pharmaceutical composition containing the compounds, and application of the compounds to preparation of medicines for preventing and/or treating peptic ulcer.
US20100167993 Compounds for Enhancing p21 Expression and Methods of Use Thereof The present invention relates to a method for identifying a drug candidate for enhancing expression of p21ctpl/wafl in a human patient suffering from a medical condition that can be treated by enhancing expression of p21Cφl/wafl. The method includes (a) providing a cell line comprising a nucleic acid sequence that comprises a p21ctpl/wafl promoter operationally ligated to a reporter domain; (b) exposing the cell line to a compound; and (c) identifying a compound that induces expression of the reporter domain. The compound that induces expression of the reporter domain is a drug candidate for treating a medical condition that can be treated by enhancing expression of p21cipl/wafl.
EP2205558B1 Substituted n-phenyl-pyrrolidinylmethylpyrrolidine amides and therapeutic use thereof as histamine h3 receptor modulators The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I) as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.
WO2011105649A1 New method for manufacturing pitavastatin hemicalcium using new intermediate The present invention is useful as a HMG-Co A reductase inhibitor and relates to a new method for manufacturing pitavastatin hemicalcium which is used as a treatment for hyperlipidemia. More specifically, a new method for manufacturing pitavastatin hemicalcium using a new intermediate is disclosed. The present invention has the following advantages: the usage of the new intermediate for manufacturing pitavastatin provides a more effective method for manufacturing pitavastatin; an alcohol protecting group, which is one of the new intermediates, easily protects dialcohol within one to two hours under acid catalyst and mild reaction conditions; the deprotection reaction of dialcohol is completed within thirty minutes to one hour under very mild reaction conditions of 0 to 25 degrees celsius, which reduces the formation of isomers to the extent possible. Also, the present invention is able to obtain a high yield of high purity pitavastatin hemicalcium despite consecutively executing a hydrolytic reaction and a pitavastatin hemicalcium reaction, without an isolation reaction after the deprotection reaction.
CN103690937A Children oral decayed-tooth spray containing marine biological ingredients and preparation method thereof The invention discloses children oral decayed-tooth spray containing marine biological ingredients and a preparation method thereof. The children oral decayed-tooth spray containing the marine biological ingredients disclosed by the invention comprises the following components in percentage by weight: 10-15% of xylitol, 6-10% of algal polysaccharides, 3-8% of chitin, 5-8% of marine biologic enzyme, 5-10% of animal antimicrobial peptide, 0.05-1% of edible essence, and the balance of purified water. Because of containing the natural marine biological ingredients, the children oral decayed-tooth spray containing the marine biological ingredients disclosed by the invention is free from toxic and side effects, obvious in antibacterial and anti-inflammatory effects and convenient for use by being uniformly sprayed on the surface of teeth and is capable of eliminating malignant bacteria of oral inflammation, keeping oral flora balance and treating ulcer and inflammation rapidly and moderately.
WO2006137465A1 Nitrogenated heterocyclic derivative It is found that a nitrogenated heterocyclic derivative represented by the formula (I) can bind specifically to an NR1/NR2B receptor and can be used as an analgestic agent. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof or the like: (I) wherein A1 represents a nitrogenated aromatic monocyclic group or nitrogenated aromatic fused-ring group which has at least one hydroxyl and/or amino and which may be substituted by other group or a nitrogenated aromatic monocyclic ring or nitrogenated aromatic fused-ring group which has -NH- in the ring and in which other ring-constituting atom may be substituted; A2 represents an aromatic hydrocarbon cyclic group which may have a substituent or the like; R1 and R2 independently represent a hydrogen, hydroxyl or the like; m is 0 or 1; X represents a lower alkylene, -CO(CR3R4)n- or -A3-(CR3R4)n- which may have a substituent or the like; Y represents a single bond, a lower alkylene or the like; and R3 to R15 independently represent a hydrogen, a lower alkyl or the like.
CN102028935A Method for forecasting, preventing and treating septicemia and septic shock and kit The invention provides a method for forecasting, preventing and treating septicemia and septic shock and a kit, particularly a protein CRISPLD2 related to septicemia and septic shock. The invention can be used for preventing and treating septicemia and septic shock by improving the concentration of the CRISPLD2 protein in serum. The invention also discloses a corresponding CRISPLD2 protein and an application thereof as a promoting agent.
CN1676128A Carsickness medicine The present invention relates to a drug for curing car sickness, sea sickness and air sickness. It is characterized by that it includes (wt%) 10% of dimenhydrinate and 1% of anisodamine (654-2).
CN101780073A Febuxostat dispersible tablet drug and preparing method thereof The invention relates to a febuxostat dispersible tablet drug and a preparing method. The drug is prepared from febuxostat as the active drug ingredient, and acceptable auxiliary ingredients in the dispersible tablet preparation. The febuxostat dispersible tablet drug is characterized in that at least one of polyoxyethylene 40 monostearate ingredient, polyethenoxy ether castor oil ingredient and hydrogenated castor oil polyoxyl ingredient in the auxiliary ingredients is used as a solubilizing agent ingredient and has the usage amount of 0.1-5 times the weight of febuxostat. The drug can obviously enhance the dissolution rate of the insoluble effective drug ingredient of febuxostat, and has the advantages of high drug dispersion degree, high dissolution rate, quick absorption and effect taking, high biological utilization degree, and the like.
WO2009123487A1 Compounds for treating pain The present invention relates to a compound of formula I (I) wherein X is hydrogen, R1, RIC(O), R1C02, or a C0X2 inhibitor, wherein R1 is C1-20 alkyl, aryl, arylalkyl, alkyloxy or arylalkyloxy; wherein Y is 0R2, NHR3 N(R3)2, or a COX inhibitor; wherein R2 is hydrogen or C1-20 alkyl and each R3 is independently hydrogen or a C1-4 alkyl; wherein T is 0R4, NHR5 N(R5)2, or a COX inhibitor; wherein R4 is hydrogen or C1-20 alkyl and each R5 is independently hydrogen or a C1-4 alkyl; wherein Z is hydrogen, R6, R6C(0), R6CO2, or a C0X2 inhibitor; wherein R6 is C1-20 alkyl, aryl, arylalkyl, alkyloxy or arylalkyloxy; with the proviso wherein when X and Z are hydrogen and T is OH, Y is not OH; for use in the prevention and/or treatment of pain wherein said compound is provided for systemic administration.
US20110256185 Reinforced tissue shields Self-reinforced tissue shields are useful as ophthalmic shields, wound dressings, wound barriers, nerve repair, therapeutic drug delivery devices and the like. The self-reinforced tissue protective shields comprise gelatin, chitosan and reinforce and are made by a method comprising forming inter-molecular locking within a solution through electrostatic forces, eliminating the use of extra cross-linking methods, the solution mainly comprising natural existing polymers that are biodegradable and biocompatible.
CN101152165A Antineoplastic isoliquirtigenin tablet The invention discloses an antitumor isoliquiritigenin tablet. The isoliquiritigenin is used as an effective component to prepare antitumor tablet. The antitumor isoliquiritigenin tablet contains isoliquiritigenin, filler, adhesive, disintegrant, wetting agen and lubricant, which are proportioned according to a certain proportion. The formula is reasonable and the use is convenient. The drug combination prepared in the method has good antitumor function, good treating effects and low side effects.
EP1771447A1 Fused pyrimidine derivatives and compositions thereof as cxcr3 receptor modulators, useful in prevention and treatment of inflammatory and immunoregulatory disorders and diseases Compounds are provided having the formula: wherein variables Ra, R1, R2, R3, R4, A1, A4, L, Q, X and subscript n as described herein. The subject compounds are useful for treatment of inflammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.
CN101186936A Method for producing dry bacterium powder containing gamma-linolenic acid The invention discloses a process for producing dry bacterial powder which contains gamma-linolenic acid, comprising the following steps of screening strain, inclined surface vibrating culture, multi-stage fermentation, filtering, dehydration, drying, crushing and packaging. Further, the improvement of the invention is that the dying procedure is realized under the condition of -40 to 30 DEG C. The specific process includes that the vibrating drying is proceeded on the condition of 20-30 DEG C and 0.4-0.6 Pascal, or the drying is proceeded by utilizing air of which the moisture degree is 20% to 30% in the manner of vibration under the condition of -40 to 20 DEG C. The invention ensures the survival rate of bacterium through improving the drying art, thereby guaranteeing the quality of gamma-linolenic acid, and improving the quality of the final product. The invention also provides the specific art parameter of each procedure and is capable of further ensuring the achievement of fine-quality products.
EP2305222A1 Compositions and methods for enhancing the antioxidant status of animals Compositions suitable for enhancing the antioxidant status of animals containing methionine, taurine, vitamin C, and vitamin E and methods for preparing and using such compositions to enhance the antioxidant status of animals are disclosed.
CN101822655A Baby nasal spray and preparation method thereof The invention relates to a baby nasal spray and a preparation method thereof, belonging to the technical field of medical health care. The preparation method comprises the following steps of: respectively preparing xylitol/xylose and sodium chloride into 5-90% solution and 0.5-10% solution according to the weight percentage, mixing the two solution according to the amount of dry mass ratio of 5-65:1, adding 0.01-0.1% benzalkonium chloride or 0.001-0.1% benzyl alcohol according to the weight percentage as a preservative, and uniformly stirring at 20-80 DEG C to obtain the nasal spray. The nasal spray prepared by adopting the xylitol saline solution can effectively treat nasopharyngitis, reduce the infectious dose of nasopharyngitis bacteria, can not generate resistance, can reduce the dependence on antibiotic, effectively prevents otitis and sinusitis and remarkably improves asthma caused by infection of the upper respiratory tract.
WO2008099426A1 A composition for selective serotonin reuptake inhibition and process thereof The present invention relates to a novelsynergistic pharmaceutical composition for serotonin reuptake inhibition, wherein thesaid composition comprises pentacyclic terpenoid glycosides, preferably asiaticoside and madecassoside optionally along with excipients. Also the present invention relates toexcipients; a process of preparation of novelsynergistic pharmaceutical composition for serotonin reuptake inhibition, wherein the process comprising steps of: (a) obtaining extract from the plant Centella asiatica; (b) treating the extract with the solvents to remove fatty substances, chlorophyll and other colorants; (c) purifying the extract through HPLC to obtain the eluted solvent; and (d) concentrating the eluted solvent to arrive at the composition. The invention also relates to thecomposition; and use of a composition comprising pentacyclic terpenoid glycosides, preferably asiaticoside and madecassoside optionally along with excipients to manufacture a medicament for serotonin reuptake inhibition in a subject in need thereof.
WO2013093931A3 Novel prodrugs of phenolic drugs The present invention relates to novel hydrazide group containing carbamate prodrugs of phenolic drugs of formula (I) or pharmaceutically acceptable salt thereof, and process for the preparation thereof.
US20050085644 Antidiabetic agents; insulin resistance Compound of formula (I): wherein: R1 and R2, which may be identical or different, each represents hydrogen, acyl or alkyl, Ar represents aryl or heteroaryl, A represents a group selected from: R4 represents hydrogen or alkyl, R5 represents hydrogen, alkyl, aryl or heteroaryl, R3 represents aryl, heteroaryl, dicyclopropylmethyl or benzhydryl, or A-R3 represents an optionally substituted naphthyl group, with the exclusion of 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-phenylethenyl)-1,4-benzoquinone, 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-naphthyl)-1,4-benzoquinone and 2,5-dihydroxy-3-(2-naphthyl)-6-phenyl-1,4-benzoquinone. Medicinal products containing the same which are useful in the treatment of diseases associated with a deregulation of glycaemia.
US20110300220 Solid calcium lactate in substantially spherical form Solid calcium lactate in the form of substantially spherical particles, characterised in that the spherical particles have a particle size distribution such that most of the particles are between 280 and 550 microns in size and the calcium lactate can be rapidly dissolved in water.
CA2290521C Medicinal aerosol products A pharmaceutical aerosol formulation suitable for oral and/or nasal inhalation including the anti-inflammatory drug ciclesonide, hydrofluorocarbon propellants such as HFC 134a and/or 227, and ethanol in an amount sufficient to solubilize the ciclesonide (and various optional ingredients, such as surfactant). The formulations exhibit very desirable physical and chemical stability, as well as excellent delivery characteristics.
CN102274238B Pharmaceutical composition for treating pancreatic cancer The invention discloses a pharmaceutical composition for treating pancreatic cancer, and the pharmaceutical composition comprises gemcitabine and tetrahydropyrimidine or tetrahydropyrimidine derivatives used as active ingredients, wherein the tetrahydropyrimidine derivatives include 1,4,5,6-tetrahydro-2-methyl-5-hydroxy-4-pyrimidinecarboxylic acid and the like. The mass ratio of gemcitabine to tetrahydropyrimidine or tetrahydropyrimidine derivatives in the composition is 3:1. The inventor found in pharmacodynamic studies that the combination of gemcitabine and tetrahydropyrimidine or tetrahydropyrimidine derivatives in a certain proportion has distinct therapeutic effect on pancreatic cancer. Tetrahydropyrimidine or tetrahydropyrimidine derivatives can improve the therapeutic effect of gemcitabine on pancreatic cancer, and can reduce the toxicity of gemcitabine.
US20070025913 Immunoglobulin which specifically binds endothelial cell-specific polypeptides; for use as evaluative tool in immunodiagnostic and drug efficacy studies The present invention relates to endothelial cell-specific genes and encoded polypeptides and materials and uses thereof in the imaging, diagnosis and treatment of conditions involving the vascular endothelium.
CN102086239A Preparation method of silkworm chrysalis chitosan derivatives with anticoagulation activities The invention relates to a preparation method of silkworm chrysalis chitosan derivatives CS-B-R with anticoagulation activities, wherein the CS is a chitosan molecule which is extracted from the silkworm chrysalis and contains active groups such as -NH2, -OH and the like; B is a linking group such as a propyl group, an ethyl group and the like; R is a molecule chain section which contains -NH, -COOH and the like and can be subjected to complexing with calcium ions. The preparation method is as follows: preparing an intermediate with a halogenation activity by using corresponding amino acid and epoxy chloropropane or ethylene hydrocarbon; and reacting the intermediate with the chitosan extracted from the silkworm chrysalis so as to obtain the product. The derivatives are simple in preparation process, can be directly dissolved in water and have the advantages of good anticoagulation effect, good biocompatibility and wide medicine application prospect.
CN102058655A Medicine for treatment of gastric disease The invention discloses a medicine for the treatment of a gastric disease, which is prepared from furazolidone, liquorice and cortex ilicis rotundae on the basis of the combination of Chinese and Western medicines, has no toxic and side effects and is moderate in nature, sweet in taste and not cold and hot. After the medicine is taken, gastric juice and gastric mucosa can be dissipated to lead the medicine to direct contact with focus of disease, thereby achieving the treating effect.
US20070011754 Lysosomal proteins produced in the milk of transgenic animals The invention provides transgenic nonhuman mammals producing phosphorylated lysosomal proteins in their milk, and methods of generating the same. Phosphorylation occurs at the 6′ position of a mannose side chain residue. Also provided are methods of purifying lysosomal proteins from milk, and incorporating the proteins into pharmaceutical compositions for use in enzyme replacement therapy.
CN103284999A Application of effective part of ramulus mori alkaloid in preparation of hypoglycemic drug The invention relates to a faint yellow powder which is provided with an effective part with hypoglycemic activity, and is prepared by smashing the ramulus mori, extracting the ramulus mori by water and/or alcohol, or extracting the ramulus mori by acid water, decontaminating in an alcohol deposition or flocculation way, concentrating, and separating and refining by a resin chromatography method. The effective part of the faint yellow powder provided by the invention, namely a hypoglycemic active ingredient, is a group of polyhydroxy alkaloids. The test by a HPLC (high performance liquid chromatography) method shows that the weight percentage of the total alkaloid in the effective part is more than 50%. The hypoglycemic dosage is 12.5-200mg for each person at every turn (by total alkaloid).
EP2323993A2 2,6-diamino- pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors The present invention is directed to compounds of formula I-V and tattooers thereof or pharmaceutically acceptable salts, esters, and pro drugs thereof which are inhibitors of sky kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
US20050234094 Inhibition of protein kinases with piridinylimidazoles a method of inhibiting a protein kinase that has a threonine or less bulky residue at the position equivalent to Thr 106 in SAPK2a/p38, and not mammalian SAPK2a/p38 or SAPK2b/p38β2, is provided, wherein the protein kinase is exposed to a pyridinyl imidazole inhibitor. The protein kinase may be a TGFβ type-I or type-II receptor.
US20100209382 Polyphenol Conjugates as RGD-Binding Compounds and Methods of Use Provided herein are compositions and methods for preventing and treating diseases and risk factors associated with metabolic syndrome by targeting the RGD-binding site of selected intra- and extracellular proteins. Exemplary compositions include RGD-polyphenol conjugates via an ester linkage; polyphenol polymer conjugated to RGD analogs or mimetics; and RGD polymer conjugates linked to polyphenol.
WO2009007110A2 Combination of benzyl-4,5-dihydro-1h-imidazole derivative and an opiod recptor ligand The present invention refers to a combination of a Compound A, a benzyl-4,5-dihydro-1H-imidazole derivative according to formula (I) and a Compound B, an opioid receptor ligand; especially of xylometazoline or oxymetazoline and a μ-opioid receptor agonist, most preferably of xylometazoline or oxymetazoline and morphine; a medicament comprising this combination; a pharmaceutical formulation for nasal application comprising this combination; or the use of this combination for the treatment of the symptoms of pain, or the prevention or the prophylaxis of the symptoms of pain, whereas pain particularily encompasses visceral pain, chronic pain, cancer pain, acute pain or neuropathic pain, specifically involving also breakthrough pain.
WO2009141627A1 Treating niemann-pick disease type c and related disorders by elevating intracellular calcium The present invention provides a compound which elevates intracellular calcium for use in the treatment of a disease which has a Niemann-Pick disease type C like cellular phenotype. The invention further provides a compound which reduces sphingosine storage for use in the treatment of Niemann-Pick disease type C.
CN1985990A Composition and application of novel medicine package for preventing and treating women's cervical virus infection The present invention is one novel medicine package for preventing and treating women's cervical virus infection, and the medicine package has novel medicine recipe, novel medicine form and novel medicine transfer device. The medicine package is for treating chronic cervicitis caused by sexually transmitted cervical human papilloma virus (HPV), herpes simplex virus II (HSV-2), cytomegalovirus (CMV), etc and cervical epithelium maldevelopment. It has the functions of inhibiting virus propagation and preventing cervical carcinoma. The present invention has unique medicine recipe, special medicine transfer mode, accurate administration to the pathological cervical part, high local medicine concentration, lasting medicine action period and raised antiviral effect. The cervical Papanicolaou smear examination reveals that the present invention is advance and effective.
CA2372206C Novel crystalline forms of a macrolide antibiotic Novel crystalline forms of a compound of formula (1) are disclosed. Also disclosed are pharmaceutical compositions comprising theses forms, and methods of their preparation and use.
CN101862312A New application of 6-gingerol The invention discloses new application of 6-gingerol. The 6-gingerol is used for respectively regulating M8 and V1 subtype transient receptor potential ion channels (short for TRPM8 and TRPV1) of mammals including humans and can be also used for preparing medicaments for treating related diseases, such as cryalgesia allergy, the parkinsonism, painful bladder syndrome, chronic obstructive pulmonary diseases, and the like as well as tumors of skin, the prostate gland, the mammary gland, the lung, the colon, and the like, participated by the ion channels. The action intensity of the 6-gingerol is higher than that of capsaicin.
EP1501806B1 Preparations for the topical application of anti-androgenically active substances Disclosed is a preparation containing at least one form of lipid nanoparticles or a nanoemulsion, containing at least one compound of formula I and/or a stereoisomeric form of the compound of formula I, in which R1 represents -(C5-C17) alkyl or -(C5-C17) alkenyl. Said preparation is suitable for treating androgenetic alopecia, hirsutism, i.e. the prevention of undesired hair growth, seborrhoea, and acne and can also be used in cosmetics.
EP1439174B1 4-IMIDAZOLIN-2-ONE COMPOUNDS AS p38 MAP KINASE INHIBITORS Compounds represented by the general formula [|] or pharmacologically acceptable salts thereof: [|] wherein G1 is halogeno, alkyl which may be substituted with alkoxy, or a group represented by the general formula [||]: [||] (wherein B is optionally substituted benzene or the like; and W is a single bond or C1-4 alkylene which may be substituted with one or two alkyl groups); Q1 and Q2 may be the same or different and are each hydrogen, halogeno, or alkyl; n is 0, 1, 2, 3, or 4; R1 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted phenyl, or the like; Z1, Z2, Z3, and Z4 may be the same or different and are each CH or N, with the proviso that three or more of Z1, Z2, Z3, and Z4 are not simultaneously N; G2 is hydrogen, -NR3R4, -OR5, or the like; and R3 to R8 are each independently hydrogen, optionally substituted alkyl, alkenyl, alkynyl, or the like.
CN103157110A Application of aromatase inhibitor in preparation of anti-cirrhosis or anti-liver fibrosis drugs The invention relates to application of an aromatase inhibitor in preparation of anti-cirrhosis or anti-liver fibrosis drugs. The aromatase inhibitor particularly can be exemestane, formestane, letrozole or anastrozole, and they can all reach good effects in anti-fibrosis and anti-cirrhosis aspects.
CN101235038B Use of glycyrol in preparing immunity inhibitor A new immunosuppressive agent as glycyrol has significant immunosuppressive activity, thus is useful as an immunosuppressive agent to treat relative diseases, wherein the glycyrol is a coumestrol compound extracted from glycyrrhiza, which is a small molecular compound with novel chemical structure. Tests prove that the glycyrol can inhibit the increment of T lymphocyte induced by canavaline A and inhibit one-way mixed lymphocyte reaction (MLR), release the inflammatory symptom of delayed hypersensitivity and inhibit the homologous allogenic organ transplantation rejection. The glycyrol is a high-effective low-toxicity immunosuppressive agent, with small molecular weight and simple structure, which is easy to be modified and to prepare different drug agents, therefore, the compound is a new generation immunosuppressive agent.
CA2356151C Triazineone compounds for treating diseases due to sarcosystis, neospora and toxoplasma Disclosed herein are methods of treating therapeutically, or metaphylactically infected animals susceptible to, or infected animal suffering from parasitic neurologic or abortigenic diseases due to Sarcocystis, Neospora or Toxoplasma that are treatable with triazineone compounds by administering thereto a pharmaceutically effective amount of the compound, including a single high dose therapeutic treatment.
US20100104555 HCV neutralizing epitopes The invention relates to modified hepatitis C virus E2 polypeptides that are effective in eliciting the production of cross-neutralizing antibodies against hepatitis C virus. The invention provides modified hepatitis C virus E2 polypeptides, preparations and pharmaceutical compositions containing them, as well as methods for using these modified E2 polypeptides.
US20130272998 Polynucleotide constructs, pharmaceutical compositions and methods for targeted downregulations of angiogenesis and anticancer therapy A novel nucleic acid construct for down-regulating angiogenesis in a tissue of a subject is provided. The nucleic acid construct includes: (a) a first polynucleotide region encoding a chimeric polypeptide including a ligand binding domain fused to an effector domain of an apoptosis signaling molecule; and (b) a second polynucleotide region encoding a cis acting regulatory element being for directing expression of the chimeric polypeptide in a specific tissue or cell; wherein the ligand binding domain is selected such that it is capable of binding a ligand present in the specific tissue or cell, whereas binding of the ligand to the ligand binding domain activates the effector domain of the apoptosis signaling molecule. Also provided are methods of utilizing this nucleic acid construct for treating diseases characterized by excessive or aberrant neo-vascularization or cell growth.
EP2709607A1 A water soluble composition comprising curcumin having enhanced bioavailability and process thereof The invention disclosed relates to a water-soluble composition having enhanced bioavailability useful for the treatment of depression which comprises a synergistic combination of curcumin, at least an antioxidant, a hydrophilic carrier and a fat. The invention also discloses a process for the preparation of the curcumin composition which comprises the steps of dissolving curcumin, at least one antioxidant, a hydrophilic carrier and a fat in a solvent to form a homogenous mass; warming the resultant mass at a temperature ranging from 25°C to 60°C for a period of 4 to 8 hours to obtain a dry wet mass; removing the solvent by evaporation to form dry mass and pulverizing the dry mass to form a fine powder.
CN101991590A Stilbene glucoside medical composite and preparation method thereof The invention relates to a stilbene glucoside medical composite and a preparation method thereof. The stability of the medical composite in the solid state or the liquid state is greatly improved; and the preparation method is convenient and feasible and is suitable for industrial production.
US20100173882 Steroidal Compositions Provided herein are steroid containing compositions suitable for providing therapeutically effective amounts of at least one steroid to individuals. Also provided herein are compositions comprising testosterone and/or testosterone derivatives suitable for providing therapeutically effective and safe amounts of testosterone over periods of time. Further provided are methods of treating andro- and/or testosterone deficiency in individuals by administering to the individuals compositions described herein.
CN102552117A Injection containing ibuprofen and preparation method of injection The invention relates to an injection containing ibuprofen and a preparation method of the injection. A metal ion chelator in the injection is ethylene diamine tetraacetic acid disodium or ethylene diamine tetraacetic acid calcium sodium; small white spots and an ibuprofen injection of which the number of visible foreign matters is remarkably reduced can be obtained by controlling the weight percentage of the metal ion chelator to be 0.05-0.48 percent; and when an internal coating material of the injection is neutral borosilicate glass ampoule, an ibuprofen injection with stable quality and favorable clarity can be obtained; and the problem that the visible foreign matters are easily generated in the large-scale industrial production of the domestic ibuprofen injection at present is solved. In addition, the injection is simple in production process, controllable in quality and is more suitable for industrial production.
US20050043222 Pharmaceutical combinations comprising a fungicide, a bacteriostatic sulphonamide and an antibacterial compound for topical application Medical combination and its method of topical use comprising active ingredients which are sparingly soluble in water, preferably in one single composition against microbes which are pathogenic in humans and animals and which usually appear together. It comprises at least one active ingredient which is effective against several of the opportunally pathogenic strains of the group consisting of fungi Candida, Aspergillus, and/or Fusarium, and aerobic bacteria: Gram-negative bacilli such as Proteus, Pseudomonas, enterobacter species, Escherichia coli, Klebsiella, Serratia marcescens, Citrobacter, Aeromonas; Gram-negative cocci such as Neisseria, Acinetobacter species; Gram-positive bacilli such as Corynebacterium speies, Bacillus sphaericus, Gram-positive cocci such as Streptococcus species; anaerobic bacteria: Gram-negative cocci such as Bacteroides, Fusobacteria; Gram-positive cocci such as Peptococcus, Peptostreptococcus species; Gram-positive bacilli such as Clostridium, Propionibacterium, Eubacterium species and Mycobacterium species suh as Mycobacterium ulcerans, microbes similar to bacteria of the Chlamydia species such as Chlamydia trachomatis. To be used for treatment of the skin or mucous membranes bearing epithelial lesions, deficiency or injuries and to be used in body cavities to prevent or cure infections and deficiencies. The composition contains-dispersed in a carrier which is pharmaceutically acceptable on the site of treatment-at least one fungicide, which is preferably azole or polyene type and at least one antibacterial compound preferably of the erythromycin, azalide, linkozamide, polypeptide type and at least one bacteriostatic sulphonamide. Additionals mainly for use on skin may include zinc oxide and asulene. Useful in forms of ointment, tablet, effervescent tablet, suppository, foam.
EP1102838B1 A method of modulating the efficiency of translation termination and degradation of aberrant mrna involving a surveillance complex comprising human upf1p, eucaryotic release factor 1 and eucaryotic release factor 3 This invention provides a method of modulating translation termination efficiency of mRNA and/or promoting degradation of aberrant transcripts. Also, this invention provides a method of screening for a drug active involved in enhancing translation termination and a method for identifying a disease state involving defective the protein complex. This invention provides a purified complex comprising an amount of a human Upflp protein, a peptidyl eucaryotic release factor 1 (eRF1) and a peptidyl eucaryotic release factor 3 (eRF3) effective to modulate translation termination. Further, this invention provides an expression vector which comprises a nucleic acid encoding a human Upflp protein, a peptidyl eucaryotic release factor 1 (eRF1) and a peptidyl eucaryotic release factor 3 (eRF3) operably linked to a regulatory element. This invention provides an antibody which binds to the complex comprising an amount of a human Upflp protein, a peptidyl eucaryotic release factor 1 (eRF1) and a peptidyl eucaryotic release factor 3 (eRF3)effective to modulate translation termination. This invention provides an agent which inhibits or modulates the binding of human Upflp to eRF1 or eRF3. The agent may inhibit or facilitate the binding of human Upflp to eRF1 or eRF3.
CN102716148A Preparation method of copper and zinc coordination compound of urocanic acid/attapulgite based antibacterial agent and applications thereof The invention discloses a preparation method of a copper and zinc coordination compound of urocanic acid/attapulgite based antibacterial agent and applications thereof, wherein the preparation method comprises the following steps: A1. the preparation of amino attapulgit; A2. the preparation of urocanic acid/attapulgite; and A3. the preparation of the urocanic acid Cu2<+>, Zn2<+> coordination compound/attapulgite antibacterial agent. The urocanic acid coordination compound/attapulgite antibacterial agent has favorable antibacterial effect on escherichia coli, and the antibacterial effect is relatively stable; the mass concentration is 3g/L, the antibacterial ratio of escherichia coli for 24 hours by zinc coordination compound of urocanic acid/attapulgite can reach 98%, and the antibacterial ratio of escherichia coli for 24 hours by the copper coordination compound/attapulgite can reach 87%; and integrating the influences to human bodies by zinc and copper ions as well as the antibacterial capability of the antibacterial agent, the zinc coordinate compound of urocanic acid/attapulgite is an external applied antibacterial agent with greater develop prospect.
WO2010010934A1 Heterocyclidene derivative having p-substituted arylacetamide Disclosed are: a compound represented by formula (I) [wherein m represents a number of 0 to 2; n represents a number of 1 or 2; p represents a number of 0 to 2; q represents a number of 0 or 1; R1 represents a halogen, a C1-2 alkyl, or the like; R2 represents a halogen, a C1-5 (substituted) alkyl, or the like; R3 represents a hydrogen atom, a halogen, a (halogen-substituted) C1-6 alkyl, or the like; X1 represents O or -NR6-; X2 represents a methylene, O or -NH-; Y represents a single bond, or a (halogen-substituted) C1-4 alkylene group; G1 and G2 independently represent N or C-R7; and the moiety represented by "Cycle" represents a 5- to 6-membered aryl which may have one or two members selected from N, O and S], a salt of the compound, or a solvate of the compound or the salt; and a pharmaceutical composition and a TRPV1 receptor modulator each comprising the compound, the salt or the solvate as an active ingredient.
CN101224215B Uses of ursolic acid saponin and oleanolic acid saponin in preparing medicine for increasing white blood cell and/or blood platelet The invention provides an application of ursolic acid saponin and oleanolic acid saponin with a general formula I in the preparation of medicines for increasing leucocyte and/or blood platelet. The invention also provides a medicine combination with the chemical compound. The invention adopts the low-cost ursolic acid and oleanolic acid which is easily available from natural products and introduces monosaccharide and oligosaccharyl through structure modification. Pharmacology experiments prove that the invention can notably increase the leucocyte and/or the blood platelet.
CN103183615A Extraction method of honeysuckle chlorogenic acid and its product The invention discloses an extraction method of honeysuckle chlorogenic acid. The method provided in the invention has the advantages that: the honeysuckle raw material is processed by a superfine grinding process, the particle size distribution is uniform, the original physicochemical properties are kept, the bioavailability is high, a freshness retaining effect of honeysuckle can be achieved, and simultaneously the grinding process has certain sterilization function; by high speed centrifugation, loss of effective components can be effectively prevented, so that high purity honeysuckle chlorogenic acid crystals can be obtained; the high purity honeysuckle chlorogenic acid crystals obtained by a microencapsulation treatment is beneficial to long-term storage; the adding of microencapsulated catechin-tea flavonoid crystals is conducive to better playing an antibacterial and antiviral role the role; and silver ions are more in favor of bringing the sterilizing and virus-killing functions of catechin-tea flavonoid into play.
EP1423124B1 Lyophilized formulation comprising olanzapine The invention provides an amorphous, lyophilized, parenteral formulation of olanzapine.
CN101658527B Composition for suppressing target gene expression The invention relates to a composition for suppressing target gene expression, which contains siRNA as an active component that can specifically suppress the target gene expression. The composition also comprises fluoroquinolone, wherein the mol ratio of the siRNA and the fluoroquinolone is from 1:5*10<2> to 1:1*10<7>. The composition for suppressing target gene expression comprises the siRNA andthe fluoroquinolone, the fluoroquinolone can increase the efficiency of the siRNA, disclosed as a picture 3, the effective concentration of 50 percent (EC50) of enoxacin is about 30 micrometers, and therefore, the composition can more effectively suppress the target gene expression. Compared with the singly used siRNA, the composition can realize the needed suppression effect under lower siRNA concentration, thereby reducing to miss targets; moreover, in an effective concentration range, the fluoroquinolone can not influence the normal functions of cells and organisms, and therefore, the composition is safe.
US20110178180 Deuterium-enriched colchicine, thiocolchicine, and derivatives thereof; methods of preparation; and use thereof Disclosed herein are deuterium-enriched colchicine, thiocolchicine, and derivatives thereof. The deuterium-enriched compounds are useful as, an antiproliferative agent, a muscle relaxant, an anti-inflammatory agent, or an anti-gout agent.
US20080318293 Sulfotransferase Inhibitors A galactosamine derivative represented by the following formula (1): wherein R1, R2 and R5 each independently represents SO3 − or H, and at least one of them represents SO3 −; R3 represents H, acetyl or SO3 −; R4 represents H, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted acyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; X represents O, S, NH or CH2; and
US20080138406 Composition for treatment of pain in bones and joints The present invention is a composition delivering effective amounts of Glucosamine, Devils Claw, and SAM in a single dosage unit.
US20050176826 Use of asc-1 inhibitors to treat neurological and psychiatric disorders The present invention relates to the identification and use of compounds that are inhibitors of the alanine-serine-cysteine transporter 1 (asc-1). This includes an assay for the identification of compounds that are inhibitors of asc-1, as well as pharmaceutical compositions comprising these compounds. The invention also comprises a method for the use of these compositions for the treatment, alleviation or amelioration of memory and attention deficits resulting from but not limited to Alzheimer's disease, Parkinson's disease, trauma and stroke, and for enhancement of learning and memory ability in a human not suffering from any neurological disorders. Finally, the invention comprises methods for use of the compositions for alleviation or amelioration of conditions in which there is altered glutamatergic or dopaminergic neurotransmission such as schizophrenia, Parkinson's disease, epilepsy, depression, obsessive compulsive disorders and bipolar disorders.
WO2013174863A1 Chondroitin for use in medicine Chondroitin, a metabolic intermediate of chondroitin sulphate biosynthesis in mammals and other living organisms, possesses biological properties different from those of chondroitin sulphate, and can be advantageously used for applications in the pharmaceutical, nutraceutical, cosmeceutical and medical device fields. Chondroitin has biostimulating, anti-inflammatory and antimicrobial activity and can be used in the treatment of osteoarthritis, eye disorders, interstitial cystitis, lung disorders, inflammatory disorders in general, oncological disorders, peritoneal dialysis, tissue biorevitalisation and wound repair, as a skin filler, and as bioresorbable scaffolds.
WO2014088326A1 Composition comprising phosphodiesterase type 5 inhibitor for inhibiting apoptosis of nerve cells The present invention relates to a composition and health functional food for inhibiting apoptosis of cranial nerve cells, and to a method for inhibiting apoptosis, wherein the composition and health functional food comprising a phosphodiesterase type 5 active inhibitor. According to the present invention, the PDE5 inhibitor exhibits a protective effect on nerve cells by inhibiting apoptosis of cranial nerve cells. Thus, the present invention can be effectively used to prevent, alleviate, and treat cranial nerve disease.
US20070293527 1-Methyl-1,3,4,5,6,11b-hexahydro-2H-11-oxa-4a-aza-benzo[a]fluoren-1-ol; alpha 2C adrergic receptors; adrenergic blocking agents; central nervous system; cognition activators; antidepressants; anxiolytic agents; peripheral nervous syster; antidiabetic agents; hypertensive agents; Raynaud's disease A compound of formula 1, wherein X, Z, R1 to R10, R15, R16, m, n, r and t are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2 antagonist. The compounds of formula I can be used for the treatment of diseases or conditions where antagonists of alpha-2 adrenoceptors are indicated to be effective.
WO2010048087A3 Compositions and methods for treating periodontal disease comprising clonidine, sulindac and/or fluocinolone Effective treatments of periodontal disease for extended periods of time are provided. Through the administration of an effective amount of clonidine, sulindac, and/or fluocinolone at or near a target site, one can reduce, prevent, and/or treat periodontal disease. In some embodiments, when appropriate formulations are provided within biodegradable polymers, treatment can be continued for at least two weeks to two months.
US20100152247 medicament for treating schizophrenia comprising cilostazol The invention relates to a medicament for preventing and/or treating schizophrenia which comprises as an active ingredient cilostazol or a pharmaceutically acceptable salt thereof.
US20110196015 N 1-2-thiophene-2-ylethyl-n2-substituted biguanide derivate, preparation method thereof, and pharmaceutical composition containing the same as active ingredients The present invention provides an N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.
WO2013015288A1 Lipase activity inhibitor Provided are: a lipase activity inhibitor having excellent lipase activity inhibitory action; a cosmetic containing said lipase activity inhibitor; use of a phospholipid for manufacturing said cosmetic; use of a phospholipid for manufacturing a drug, anti-acne agent, anti-obesity agent or anti-inflammatory agent containing said lipase activity inhibitor; a phospholipid for use in inhibiting lipase activity; a phospholipid for use in preventing or treating acne, obesity or inflammation; and a method for preventing or treating acne, obesity or inflammation, including administration of said phospholipids. The present invention pertains to: a lipase activity inhibitor containing a phospholipid as the active ingredient, and a cosmetic, drug, anti-acne agent, anti-obesity agent or anti-inflammatory agent containing said lipase activity inhibitor; use of a phospholipid for manufacturing said cosmetic, drug, anti-acne agent, anti-obesity agent or anti-inflammatory agent; a phospholipid for use in inhibiting lipase activity; a phospholipid for use in preventing or treating acne, obesity or inflammation; and a method for preventing or treating acne, obesity or inflammation, including administration of said phospholipids.
US20110065637 Method to reduce SLOSH energy absorption and its damaging effects through the reduction of inelastic collisions in an organism A first embodiment can be a method to reduce SLOSH energy absorption within an organism by reducing the inelastic collisions. A fluid containing organism can utilize an embodiment of the method wherein one or more of reversibly increasing pressure within the organs or cells, reversibly increasing the volume within the organs or cells, reversibly altering vascular, molecular, or cell wall stiffness, or reversibly altering vascular, molecular, or cell wall configuration within said organism may reduce these collisions.
US20090253648 Tricyclic-Nucleoside Compounds for Treating Viral Infections Disclosed are compounds represented by formulae I, II, and III, and the compositions and methods thereof for treating viral infections caused by a Flaviviridae family virus.
WO2006117696A3 Diastereoisomers of 4-hydroxyisoleucine and uses thereof The invention relates to configurational isomers 4-hydroxyisoleucine, and to lactones, pharmaceutically acceptable salts, and prodrugs thereof, to processes for their preparation, and to pharmaceutical compositions comprising the same. The isomers of the invention exhibit insulinotropic activity and thus may be useful for the prevention and treatment of disorders of carbohydrate or lipid metabolism, including diabetes mellitus (type 1 and type 2 diabetes), pre-diabetes, and Metabolic Syndrome.
CN101485887B 5-fluorouracil-sn2-phosphatidyl choline copolymer as well as preparation method and application thereof The invention relates to 5-fluorouracil-sn2-phosphatidylcholine copolymers and a preparation method and application thereof. The preparation method comprises: preparing 5-fluorouracil derivatives containing carboxyl groups, using a carboxylic group as a connecting group to covalently bond 5-fluorouracil on a sn2 site of phosphatidylcholine, and obtaining the copolymers. The copolymers have amphiphilic surface activity, can form liposome nano-capsules and a self-assembly delivery system, and can be taken as an intermediate preparation formulation and further prepared into a corresponding transdermal delivery preparation such as gel. The copolymers and the delivery system of the copolymers can effectively enter focuses, and can be subjected to enzymolysis through high-expression phospholipase A2 on the focuses to metabolize active skin cancer resistant medicines, namely the 5-fluorouracil, so that the copolymers and the delivery system have the advantage of skin-targeted medication of skin cancer, overcomes the defects that the water-soluble 5-fluorouracil is not suitable for transdermal administration and has low envelop rate of liposome, easy leakage and difficult acquisition of liposome with superior transdermal carrier performance, and provides a novel medicine source for clinical medicines.
CN103340822A Vaginal expansion suppository containing econazole or econazole salt, and preparing method and detection methods thereof The invention relates to a vaginal expansion suppository containing econazole or an econazole salt. The expansion suppository comprises econazole or the econazole salt, a liposolubility matrix and an expansion carrier. When the suppository is fully expanded, a medicinal layer can be in full contact with an inner wall of a vagina, so as to prevent a medicinal liquid from outflowing. The expansion suppository also comprises a tert-butyl hydroxy compound which can prevent econazole from being oxidized so as to improve the stability of econazole. The invention also provides a preparation method and detection methods of the expansion suppository. The vaginal expansion suppository containing econazole or the econazole salt employs seven original leading technologies, and also has the beneficial effects that: the expansion suppository prevents the medicinal liquid from outflowing, has high stability and lasting effect of treatment, and prevents secondary infection.
US7435726 Thalidomide and a topoisomerase inhibitor anticancer drug such as irinotecan; reduces toxicity related side effects of anticancer drug This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a pharmaceutically acceptable salt, solvate, or clathrate thereof, and irinotecan. The invention also relates to methods of treating or preventing cancer which comprise the administration of a thalidomide and another anti-cancer drug to a patient in need of such treatment or prevention. The invention further relates to methods of reducing or avoiding adverse side effects associated with the administration of chemotherapy or radiation therapy which comprise the administration of thalidomide to a patient in need of such reduction or avoidance.
US20120264775 Oligomer-Opioid Agonist Conjugates The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
EP1539121A2 Methods of promoting osteogenesis The invention is directed to methods of bone healing by administering a p38 MAP kinase inhibitor. The invention is directed to methods of treating bone fractures, bone diseases, bone grafting, especially enhancing bone healing following facial reconstruction, maxillary reconstruction, mandibular reconstruction or tooth extraction, enhancing long bone extension, enhancing prosthetic ingrowth, and increasing bone synostosis by administering a p38 MAP kinase inhibitor.
CN1651395B Borneol fatly acid ester derivative and preparation containing said derivative A derivative of the borneol ester of fatty acid, which is a target auxiliary of the medicine for treating cerebral diseases, is prepared through esterifying reaction between borneol or isoborneol and the straight-chain or branch-chani C5-C30 fatty acid.
CN102206179A Bipyridine alkaloid compound and preparation method and use thereof The invention relates to bipyridine alkaloid compounds and a preparation method and use thereof. The compounds with novel structures are produced by Actinoalloteichus sp.WH1-2216-6 separated from a marine sample. Experiments prove that the compounds can serve as cell proliferation inhibitor or antineoplastic agent.
WO2013120888A3 Core sheath drug delivery devices It relates to a device comprising (a) a core comprising polyurethane; (b) a sheath comprising ethylene vinyl acetate copolymer, said sheath substantially or completely surrounding said core; and (c) one or more active pharmaceutical ingredients dissolved or dispersed in said core and/or said sheath; and to a process for its preparation.
WO2011049825A1 Derivatives of purine or deazapurine useful for the treatment of (inter alia) viral infections The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.
CN1927185A Maleic acid trimebutine slow release tablet comprising quick release part and preparing method thereof This invention concerns a the maleic acid trimebutine sustained-releasing tablets with rapid releasing part and preparation of pharmaceutical pharmaceuticals, including double slice and tablet mixed and suppressed by particles with different releasing characteristics, it is found in the invention that after the maleic acid trimebutine and fumaric acid being mixed and granulated, the stability and compressibility of the maleic acid trimebutine is improved, and its citation moist is lowered, and it can be used for preparation of the praeparatum of the present invention, the present invention includes the rapid releasing part and sustained-releasing part.
US20080253995 For treatment of Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and rhinovirus infection The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2′R)-2′-deoxy-2′-fluoro-2′-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.
WO2009002977A1 Salacia cuspidata extract and methods of extracting and using such extract A method of inhibiting COX-2, inhibiting NF-Kappa B activation, treating inflammation, or treating cancer may comprise administering a therapeutically effective amount of an extract of Salacia cuspidata to a patient. A medicament as described herein may comprise a pharmaceutically acceptable vehicle and a therapeutically effective amount of an extract of Salacia cuspidata suspended in the vehicle. A method of making an extract of Salacia cuspidata may comprise creating a component solution by treating Salacia cuspidata material with an extractor and a solvent and producing an extract by at least partially removing liquid from the component solution. An extract of Salacia cuspidata may comprise components extracted using various solvents.
WO2011058923A1 Antibacterial agent for drug-resistant bacteria, method for screening for same, and use of same An antibacterial agent for drug-resistant bacteria, which comprises either nibomycin and/or a derivative thereof and is effective on drug-resistant bacteria each having resistance to at least one drug.
CN101991642A Walnut ointment preparation method The invention relates to a walnut ointment preparation method, which comprises the flowing steps of: steaming big walnut kernels, sesame oil and white sugar; grinding the materials into paste; sufficiently stirring the paste; and filling the materials into a container to be sealed. The walnut ointment has good effect on various kinds of calculus, is simple and convenient to use, can be easily implemented and has no toxic or side effect.
CN102665727A Anti-cancer agent Disclosed is an anti-cancer agent characterized by comprising at least one phosphine transition metal complex selected from compounds respectively represented by formulae (1a) to (1c). The anti-cancer agent has an equivalent anti-cancer activity to those of conventional anti-cancer agents and has low toxicity. [In the formulae, R1 and R2 independently represent a linear or branched alkyl group, a cycloalkyl group, a cyclcoalkyl group having a substituent, an adamantyl group, a phenyl group, or a phenyl group having a substituent, wherein each of R1 and R2 has 1 to 10 carbon atoms, R1 and R2 are different from each other, and R1 has a higher priority than R2 as ranked in accordance with the RS system; R3 and R4 independently represent a hydrogen atom, or a linear or branched alkyl group, wherein each of R3 and R4 has 1 to 6 carbon atoms, R3 and R4 may be the same as or different from each other, R3 and R4 may together form a saturated or unsaturated ring that may have a substituent; M represents a transition metal atom selected from the group consisting of gold, copper and silver; and X- represents an anion.
EP1165061B1 Use of compound preparation made of vitamin d metabolites or vitamin d analogues and partial estrogen agonists for treating osteoporosis Disclosed is a compound preparation wherein the bone cell activator is a vitamin D metabolite or vitamin D analogue and the resorption inhibitor is an oestrogenic compound. The inventive compound preparation is used in a therapeutical plan which comprises one or more cycles. Each cycle consists of the following steps: a) daily administration of a vitamin D metabolite or vitamin D analogue during 1-7 days, b) daily administration of an oestrogenic compound during 21-120 days after a) or after an interphase of up to 30 days.
EP2558468A1 5, 7-substituted-imidazo [1, 2-c]pyrimidines as inhibitors of jak kinases Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
US20090163479 Use of taurolidine to treat tumors The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing taurolidine, taurultam, or a biologically active derivative thereof. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis.
CN102552237A Medicine composition and health food for resisting liver fibrosis or cirrhosis The present invention provides a medicine composition and a health food for resisting liver fibrosis or cirrhosis, comprising an active component, for example (xanthone derivative), and an admissible carrier.
US20090042964 Amino-5-[substituted-4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds as beta-secretase inhibitors The present invention provides a 2-amino-5-[substituted-4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
US20080076175 Generating transgenic lymphoid cell comprising sequences coding immunoglobulin epitope for use in tissue targeted therapies The invention provides a method for stimulating an immune response by administering to a lymphoid cells either in a lymphoid organ or ex vivo, a nucleic acid molecule comprising a hematopoietic cell-specific expression element operationally linked to a nucleic acid sequence encoding one or more heterologous epitopes. The heterologous epitope can be inserted into a complementarity-determining region of an immunoglobulin molecule. The invention also provides a nucleic acid molecule comprising a hematopoietic cell-specific expression element operationally linked to a nucleic acid sequence encoding a heterologous polypeptide. The invention additionally provides a method of treating a condition by administering a nucleic acid molecule comprising a hematopoietic cell-specific expression element operationally linked to a nucleic acid sequence encoding a heterologous polypeptide, wherein the nucleic acid molecule is targeted to a hematopoietic cell.
CN101732481A Medicament for treating infectious swine streptococcosis The invention relates to a medicament, which has great effects of treating infectious swine streptococcosis, quickly clearing heat and detoxicating, cooling blood and eliminating dampness, eliminating vexation and engendering liquid, promoting recovery, and preventing secondary infection and other diseases. The medicament has the advantages of exact curative effect, no residue, no toxic or side effects, high safety, and green environmentally-friendly preparation, and is favorable for healthy development of animal husbandry.
CA2606515C Method of improving learning and memory in mammals A method of improving learning and/or memory behavior in a mammal is described which involves administering to the mammal casein glycomacropeptide in an amount sufficient to improve learning and/or memory behavior in the mammal.
US20110269797 Anln protein as an endocrine treatment predictive factor The present invention provides methods, uses and means for breast cancer prognostics and treatment prediction. Provided methods comprises the steps of: providing a sample earlier obtained from a breast cancer subject; evaluating the amount of ANLN protein present in at least part of said sample, and determining a sample value corresponding to said amount; comparing the sample value with a reference value; and, if said sample value is higher than said reference value, concluding that the subject is not likely to benefit from an endocrine treatment or that a prognosis for said subject is worse than a reference prognosis associated with the reference value.
EP1509523B1 Triazaspiro compounds useful for treating or preventing pain Triazaspiro Compounds, compositions comprising a Triazaspiro Compound, methods for treating or preventing pain in an animal comprising administering to an animal in need thereof an effective amount of a Triazaspiro Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a Triazaspiro Compound are disclosed.
US20110229408 Sodium-iodide symporter gene repressor binding site The present disclosure relates to a sodium iodide symporter (NIS)-repressor binding sites (NRBS) consensus sequence consisting of a DNA molecule having the sequence 5′-T/C(G/A)GCCT(T/C)A(G/A)TTTCCCCA(T/C)CTGT-3′(the “consensus NRBS”). The disclosure further relates to methods of restoring iodide transport in dedifferentiated thyroid cancer cells by interfering with formation or function of the NIS repressor.
WO2012055840A1 Composition and preparation for treatment of dysmenorrhea and menstrual pain and use of a hormonal agent and a zinc salt for treatment of menstrual disorders The inventions refers to a pharmaceutical composition and a preparation (regime) containing a hormone and a biocompatible zinc salt, as well as the use of a zinc salt and a contraceptive active hormone for the treatment of menstrual disorders, in particular to alleviate dysmenorrhea.
EP1480976B1 Thiazole derivatives as npy receptor antagonists Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, n, m and A have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
CN1839843A Fluorouracil slow release injection Disclosed is a 5-FU slow release injection comprising slow release microballoons and dissolvent, wherein the slow release microballoons include anti-cancer active constituent and slow release adjuvant, the dissolvent being common dissolvent or dissolvent containing suspending agent selected from sodium carboxymethylcellulose, mannitol, sorbitol, Tween-80 or their combination. The anticancer active constituent being 5-FU and/or 5-FU synergistic agent selected from antimitotic drugs and/or alkyl agent, the slow release adjuvant being selected from polylactic acid, ethylene-vinyl acetate copolymer, Polifeprosan, FAD and sebacic acid copolymer, polyglycolic acid and glycollic acid copolymer or their combination.
EP2574336A1 Use of dipeptidylpeptidase inhibitors to regulate glucose metabolism The present invention provides compositions comprising an inhibitor of dipeptidylpeptidase IV for modification and regulation of glucose and lipid metabolism, generally to reduce insulin resistance, hyperglycemia, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoprotein-emia (such as chylomicrons, VLDL and LDL), and to regulate body fat and more generally lipid stores, and, more generally, for the improvement of metabolism disorders, especially those associated with diabetes, obesity and/or atherosclerosis.
CN101555206A Angustifolia lignans, preparing method and application thereof The invention discloses an angustifolia lignans compound, a preparing method and application thereof. The compound has the right structural formula. The method comprises the following steps of: drying and crushing the rattan of schisandra angustifolia, conducting ultrasonic extraction on crushed rattan in a fractionated way by using acetone; merging and filtering extracting solution, concentrating the extracting solution into small volume in a decompression way, standing, filtering precipitates, extracting the filtered liquid for three times with ethyl acetate, and obtaining part extract liquid of the ethyl acetate, concentrating the liquid extract into an extractum, conducting chromatography and first fraction on the liquid extract with a silica gel column, then conducing further separation by adopting high-efficiency liquid phase semi-preparative chromatogram, thereby obtaining the required compound. anti-HIV-1 activity screening is conducted on the compound, and the experimental result demonstrates that the compound has good anti-HIV-1 activity and anti-oxidation activity, wherein HIV-1 therapeutic index is 22.5, and anti-oxidation median elimination concentration IC50 is 8.22 mug/L.
WO2003101177A3 Diagnosing predisposition to fat deposition and therapeutic methods for reducing fat deposition and treatment of associated conditions Provided herein are methods for prognosing and diagnosing fat deposition and related disorders (e.g., obesity and noninsulin diabetes dependent mellitus (NIDDM)) in a subject, reagents and kits for carrying out the methods, methods for identifying candidate therapeutics for reducing fat deposition and related disorders, and therapeutic methods for reducing fat deposition or treating fat deposition related disorders in a subject. These embodiments are based in part upon an analysis of polymorphic variations of the nucleic acid set forth in SEQ ID NO: 1.
US20120178775 Methods for treating frontotemporal lobar degeneration with ubiquitinated inclusions (ftld-u) Methods for rescuing learning, memory and/or motor function deficits associated with frontotemporal lobar degeneration with ubiquitinated inclusions (FTLD-U) are disclosed. The method comprises: a) administering to an animal having FTLD-U a therapeutically effective amount of an autophagy inducer; b) causing a decrease in the amount of ubiquitinated TDP-43 aggregation forms in the brain of the animal; and c) causing an improvement of the learning, memory capacities and/or motor function of the animal.
EP0977562B1 Methods and compositions for delivery of taxanes Methods and compositions for delivery of taxanes are disclosed. Particularly disclosed are compositions of taxol solubilized in Vitamin E TPGS whereby the delivery of taxol is improved.
CN102293755B Two lyophilized powder injections of methylprednisolone sodium succinate and preparation methods thereof The invention relates to two lyophilized powder injections of methylprednisolone sodium succinate and preparation methods thereof. Each lyophilized powder injection of methylprednisolone sodium succinate is obtained by dissolving 25.35-50.69mg of methylprednisolone succinate, 4.98-8.97mg of NaHCO3, 1.60mg of NaH2PO4.H2O, and 17.4mg of Na2HPO4 in water for injection, adding water for injection until 1ml, filling, and lyophilizing.
CN101810722A Composition containing gatifloxacin The invention discloses a composition containing gatifloxacin, which comprises the following components in percentage by weight: 20-30 percent of glossy ganoderma, 10-25 percent of atifloxacin, 10-15 percent of liquorice, 5-20 percent of cordyceps sinensis, 10-20 percent of saururus chinensis, 10-20 percent of plantain and 5-15 percent of starch, wherein the total weight of various components is 100 percent. The invention has the advantages of stable medicine property, remarkable therapeutic effect, quick response and low toxicity.
EP2007750A1 Azabicyclo [3. 1. 0] hexyl derivatives as modulators of dopamine d3 receptors The present invention relates to novel compounds of formula (I)' or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11 -membered heteroaryl bicyclic group; A is a group P1 or a group P2 Wherein p is an integer ranging from 0 to 5; R1 is halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1- 4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R6; and when p is an integer ranging from 2 to 5, each R1 may be the same or different; R2 is hydrogen or C1-4alkyl; n is 3, 4, 5 or 6; R6 is a moiety selected from the group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1 -dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such R6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C1- 4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1- 4alkyl, C3-7 cycloalkyl, haloC1-4alkyl, C1-4-alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR'R'; or R4 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; R5 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR'R'; or R5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; R7 is hydrogen or C1-2alkyl; R' is H, C1-4 alkyl or C1-4 alkanoyl; R' is defined as R'; R' and R' taken together with the interconnecting nitrogen atom may form a 5-, 6- membered saturated or unsaturated heterocyclic ring; wherein at least one of R4 and R5 is hydrogen; and wherein only one R2 group may be different from hydrogen; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
CN102657676A Disinfecting, vein-expanding and pain-relieving patch for skin The invention relates to a disinfecting, vein-expanding and pain-relieving patch for skin, which is used for effectively solving the problems of easiness in infecting, incapability of fully expanding blood vessels, difficulty in puncturing and large puncture pain during venous puncture infusion. According to the technical scheme of the invention, the patch is formed by uniformly mixing the following components in percentage by weight: 91-94 percent of iodine complex or alcohol, 2-3 percent of teracainum and 4-6 percent of glonoin. The patch is convenient to use, has a good effect, can be used for relieving pain, and has disinfecting and blood vessel expanding functions.
CN101822840A LIGHT-antitumor-antigen antibody for preventing and treating primary and metastatic cancer The invention relates to a tumor specific antibody linked with LIGHT protein or fragments thereof, a combination comprising the same, a method for preventing and treating cancer and application thereof. The LIGHT-antibody and combination of the invention are applicable to preventing and treating primary and/or metastatic cancer and reducing, inhibiting and decreasing primary tumor growth and/or cancer metastasis.
WO2007027133A1 7-(2-AMINO-1-HYDROXY-ETHYL)-4-HYDROXYBENZOTHIAZOL-2(3H)-ONE-DERIVATIVES AS β2 ADRENOCEPTOR AGONISTS The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4', R5', R6, R7, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
CN101104608B Solanesol derivative, preparation and application thereof The invention discloses a solanesol deriative, which refers to the compound in the following general formula. In the general formula, n is equivalent to 1-2, and R is 5-halogenated pyrimidine methy, 5-alkyl substituted pyrimidine methyl, para aromatic group substituted benzyl, or 6-alkoxy naphthalene substituted ethyl; the procedure of preparation begins when N-Solanesyl-N`-amine alkyl piperazineis dissolved in organic solvents to react 2-48 hours with raw material acid under the influence of catalysts and at the temperature of 0-25 DEG C, and is followed by column chromatography, which generates the solanesyl derivative; with no change in the solid configuration of products during the preparation, the compound, being a novel series of amide-type solanesyl derivative, retains the original all-trans configuration of solanesol units, therefore, the compound is the homologous derivative of natural products, having the activity of antineoplastic agents and the effect of antitumor synergy. The preparation procedure employed by the invention has the advantages of convenient operation, moderate conditions and high yield coeffiency and is fit for industrialization.
EP2397478A1 1,3-diaryl substituted ureas as modulators of kinase activity. Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Use in treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, or detecting a level of the activity of the angiogenic kinase.
CN1887272A Slow released dry azithromycin suspension and its prepn The present invention provides one kind of slow released dry azithromycin suspension and its preparation process. The medicine of the present invention has slow released azithromycin microsphere prepared through spray drying process, and capsule wall material for coating azithromycin medicine made of viscous medicinal polymer material or insoluble medicine polymer material, such as acrylic polymer, gelatin, Arabic gum, carboxymethyl cellulose salt, etc. and preferably of acrylic polymer. The slow released dry azithromycin suspension has improved administration compliance and convenience, and high bioavailability.
US20060079460 Purified LH Recombinant human luteinizing hormone (LH) having a specific bioactivity of from 20,522 to 31,229 IU/mg and obtainable from a process for the purification of recombinant LH from a sample of crude recombinant LH in the supernatant of CHO cells which comprises the combined use of ion-exchange chromatography and reverse phase HPLC. The ion-exchange chromatography and the reverse phase HPLC are performed twice and the final use of a gel permeation column allows the purification from any residual traces of contaminants. The recombinant LH can be formulated into a pharmaceutical composition and used for treating a fertility disorder.
US20110263714 Reverse Vesicle The reverse vesicle composition of the present invention includes (A) a sphingosine represented by formula (1) (wherein R1 represents a C4 to C30 linear alkyl group which may be substituted by a hydroxyl group, a carbonyl group, or an amino group; Y represents a methylene group, a methine group, or an oxygen atom; each of X1, X2, and X3 represents a hydrogen atom, a hydroxyl group, or an acetoxy group; X4 represents a hydrogen atom, an acetyl group, or a glyceryl group, or forms an oxo group together with the adjacent oxygen atom (wherein when Y is a methine group, one of X1 and X2 is a hydrogen atom, and the other is absent, and when X4 forms an oxo group, X3 is absent); each of R2 and R3 represents a hydrogen atom, a hydroxyl group, a hydroxymethyl group, or an acetoxymethyl group; a is a number of 2 or 3; each of (R)a represents a hydrogen atom, an amidino group, or a linear-chain alkyl group optionally having a substituent selected from among a hydroxyl group, a hydroxyalkoxy group, an alkoxy group, and an acetoxy group and containing 1 to 8 carbon atoms in total; and the broken line represents an optional unsaturated bond), (B) a C16 to C30 fatty acid, (C) a hydrocarbon oil, (D) an ester oil which is in liquid form at 25° C., and (F) water, wherein the ratio by mass of ingredient (C) to ingredient (D) satisfies the following relationship: 1≦(C)/(D)<1000, and the composition contains a surfactant having a molecular weight of 1,000 or less in an amount of 1 mass % or less.
US7872151 Inhibitors of α4 mediated cell adhesion The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof.
US8691808 Antiviral compounds and their methods of use The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.
EP2658844A1 Novel pyrimidine derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.
US6982268 Useful in the treatment of a variety of central nervous system disorders in humans including anxiety, depression, sleep disorders, attention deficit disorder, or Alzheimer's dementia Substituted imidazolylmethyl pyridine and pyrazine derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
CN101982174A Formula of compound medicine preparation for relieving cough and preventing asthma and preparation method thereof The invention relates to a formula of a compound medicine preparation for relieving cough and preventing asthma and a preparation method thereof. The formula mainly comprises the following components in parts by weight: 5-25 parts of methoxyphenamine hydrochloride, 3-15 parts of narcotine, 10-50 parts of aminophylline, 0.1-2 parts of ketotifen fumarate, and an appropriate amount of pharmaceutically acceptable auxiliary materials. In the invention, the methoxyphenamine hydrochloride, the narcotine, the aminophylline and the ketotifen fumarate are prepared into the compound medicine preparation for the first time; and the obtained compound medicine preparation has more obvious treatment effect on diseases such as cough, asthma, bronchial asthma, asthmatic bronchitis and the like; combination of the ketotifen fumarate and the aminophylline in the formula can enhance the bronchiectasis action of the aminophylline; and the mild sedation of the ketotifen fumarate can simultaneously counteract the central nervous system stimulation action caused by the aminophylline.
CN1994304A Compound orally disintegrating tablet containing loratadine and ambroxol and preparation process thereof The invention relates to a luleitadingmione oral calving tablet which can treat allergic rhinitis, etc. wherein, it has quick adsorption, high biological utilization, and simple intake method without water. It uses Loratadine and bromamine acid as materials, with some findings.
CN101775019B Melotenine and pharmaceutical composition as well as preparation method and application thereof The invention provides an active ingredient of melotenine analogue shown in the formula (I) for resisting tumour as well as a preparation method and a medical application thereof.
US7838534 muscarinic M3-receptor; respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD); 3-[(3-fluorophenyl)-(3,4,5-trifluorobenzyl)carbamoyloxy]-1-(2-oxo-2-thiophen-2-ylethyl)-1-azoniabicyclo[2.2.2]octane bromide; inhalation Quinuclidine derivative of the general formula (I) in the form of single enantiomers or mixtures thereof are useful in the manufacture of a medicament for the prevention and therapy of respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), chronic bronchitis, cough and emphysema wherein: R1 is selected from H, F, Cl, Br, I and (C1-C4)-alkyl; R2 is optionally substituted 2- or 3-thienyl, or substituted phenyl; R3 is (CH2)1-4—COR4 or (CH2)1-4—S(O)nR4, wherein R4 is optionally substituted phenyl or optionally substituted 2- or 3-thienyl; n is 0, 1 or 2; X− is a pharmaceutically acceptable anion.
CN103446124A Application of Lycojaponicumin B in small intestine peristalsis promoting drug The invention relates to application of Lycojaponicumin B in preparation of a small intestinal peristalsis promoting drug. A pharmacological experiment shows that the Lycojaponicumin B has good promoting effect on small intestinal peristalsis. The application of the Lycojaponicumin B in the preparation of the small intestinal peristalsis promoting drug is disclosed for the first time. Due to the fact that the skeleton type is a novel skeleton type and the high small intestinal peristalsis promoting activity of the Lycojaponicumin B is previously unimagined, the possibility that other compounds give any revelation does not exist, and the Lycojaponicumin B has outstanding substantive characteristics and meanwhile has a remarkable improvement in the preparation of the small intestinal peristalsis promoting drug obviously.
CN102488668A Cefuroxime axetil dispersible tablet and its preparation method The invention belongs to the medicine preparation field, more specifically relates to a Cefuroxime axetil dispersible tablet and its preparation method, the dispersible tablet comprises the following raw materials: Cefuroxime axetil, magnesium stearate, microcrystalline cellulose PH-102, aspartame, cross linked sodium carboxymethyl cellulose, essence, silica and sodium dodecyl sulfate. The method comprises the following steps: passing the above raw materials through a sieve with 40 meshes, mixing the aspartame and microcrystalline cellulose PH-102 with equal weight for 5 minutes, then adding all the cross linked sodium carboxymethyl cellulose for mixing for 5 minutes, placing the mixed powder and residual raw materials in a mixed tank, mixing for 20 minutes, tabletting by a high speed rotary tablet machine to obtain the Cefuroxime axetil dispersible tablet. The dissolution rate of the prepared Cefuroxime axetil dispersible tablet can reach more than 90% after 15 minutes, 99.5% after 45 minutes, thereby the biological availability and curative effect of the medicines can be fully enhanced.
CN102657652A Novel uses of bisbenzylisoquinoline alkaloid derivative or analogue of general formula I The invention provides a use of a bisbenzylisoquinoline alkaloid derivative or analogue to prepare medicine medicines for treating diabetic nephropathy. The bisbenzylisoquinoline alkaloid derivative of general formula I provided by the invention by relieving glomerular basement membrane thickening, reduces foot process fusion of glomerular epithelial cells and restores mechanical barrier and charge barrier of glomerulus, thus reducing protein leakage, having a good therapeutic effect on diabetic nephropathy (stage III or stage IV) patients, reducing 24h micro-albumin (UAE) and 24h urine protein (UPQ), having a good inhibitory effect on the albuminuria symptom of the diabetic nephropathy, and providing a new choice for the clinical treatment of the diabetic nephropathy.
US8603464 Alkaline phosphatase to reduce weight gain or induce weight loss The present invention provides methods for using human placental alkaline phosphatase or an active derivative to reduce blood glucose level in a mammal. Treatment regimens provided by the invention may be used to control Type 1 and Type 2 forms of diabetes in humans. The methods and treatment regimens may be effective to maintain the human's blood glucose level below about 10 mM, and preferably within the normal range of 4 mM to 7 mM. The methods and treatment regimens may be used in combination with administration of known anti-diabetic medicaments. Also provided by the invention is a method for inducing weight loss or reducing an expected weight gain caused by or associated with obesity or Type 2 diabetes. The invention further provides a preparation for administration to a human, the preparation comprising homogeneous purified human placental alkaline phosphatase in a physiologically acceptable carrier.
CN101015525A Paclitaxel liposome and preparation method therefor The invention provides a Paclitaxel liposome and process for preparation, wherein the components include Paclitaxel 1-30%, phosphatides 1-95%, cholesterin 0-30%, thermo-sensible auxiliary material D 0-50%, auxiliary material G 0-50%, freeze-drying protecting agent 0-80%, octadecyl amine 0-10%, anti-oxidant 0.001-50% and right amount of buffer salt.
EP1730144B1 Substituted 1,4,8-triazaspiro¬4.5 decan-2-one compounds The invention relates to substituted 1,4,8,-triazaspiro[4.5]decan-2-one compounds, to methods for producing said compounds, to medicaments containing said compounds and to the use of the latter for producing medicaments.
WO2006138328A1 Process for the production of antidiabetic oxazolidinediones The present invention provides a convergent process for the preparation of a family of antidiabetic phenoxy-substituted phenoxybenzyl oxazolidinediones shown as structure I. The compounds are selective PPAR gamma partial agonists (SPPARM's), which are useful in the treatment of type 2 diabetes.
WO2012036529A2 (s)-n,n-dimethyl-3-(naphthalen-1-yloxy)-1-phenylpropan-1-amine derivatives, pharmaceutical compositions containing the derivatives and manufacturing methods thereof Disclosed are novel dapoxetine derivatives and pharmaceutically acceptable salts thereof. The compounds are soluble in water, stable, and easy to process into preparations. In addition, the compounds exhibit improved dissolution rate and taste. Furthermore, the compounds exhibit a small difference in dissolution rate depending on pH. Further disclosed are pharmaceutical compositions including the compounds. The pharmaceutical compositions are useful for the treatment, management or prevention of premature ejaculation. Methods for preparing the dapoxetine derivatives are also disclosed.
WO2007024029A1 Antiviral agent and viral replication inhibitor The invention is directed to an antiviral agent which comprises a zinc finger protein and/or a nucleic acid encoding the zinc finger protein for inhibiting binding of a replication protein derived from an animal DNA virus to a replication origin of the virus.
EP2509633A2 Nanoparticle carrier systems based on poly(dl-lactic-co-glycolic acid) (plga) for photodynamic therapy (pdt) Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticutate formulations for clinical use in photodynamic therapy comprising a hydrophobic photosensitizer, poly(lactic-co-glycolic) acid and stabilizing agents are provided. These nanoparticulate pharmaceutical formulations provide therapeutically effective amounts of photosensitizer for parenteral administration. In particular, tetrapyrrole derivatives can be used as photosensitizers, whose efficacy and safety are enhanced by such nanoparticulate formulations. It also leaches the method of preparing PLGA-based nanoparticles under sterile conditions. In one of the preferred embodiments of the present invention PLGA-based nanoparticles have a mean particle size less than 500nm and the photosensitizer is temoporfϊn, 5,10,15,20-tetrakis(3-hydroxyphenyl)-chlorin (mTHPC). In another embodiment, the photosensitizer 2,3-dihydroxy-5,10,15,20-tetrakis(3- hydroxyphenyl)-chlorin (mTHPD-OH) is formulated as a nanoparticle for parenteral administration. Yet, in another embodiment preferred photosensitizer is 5,10,15,20-tetrakis(3- hydroxyphenyl)-porphyrin (mTHPP). The formulations can be used for treating hyperptasic and neoplasia conditions, inflammatory problems, and more specifically to target tumor cells.
US7375088 culture product from a Streptomyces aizunensis strain; inhibitors of fungal cell growth and cancer cell growth; for lowering serum cholesterol and other steroids This invention relates to a new class of polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for obtaining the compounds. One method of obtaining these compounds is by cultivation of novel strains of Streptomyces aizunensis; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to the novel strains of Streptomyces aizunensis used to produce these compounds, to the use of these compounds and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of fungal cell growth and cancer cell growth. The invention also relates to pharmaceutical compositions comprising these novel polyketides or a pharmaceutically acceptable salts or derivatives thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of these novel polyketides.
CA2777638A1 Genetic variants useful for risk assessment of thyroid cancer The invention discloses genetic variants that have been determined to be susceptibility variants of thyroid cancer. Methods of disease management, including methods of determining susceptibility to thyroid cancer, methods of predicting response to therapy and methods of predicting prognosis of thyroid cancer using such variants are described. The invention further relates to kits useful in the methods of the invention.
US20100035853 Method for preventing or treating cisplatin-induced nephrotoxicity Provided is a method for preventing or treating cisplatin induced nephrotoxicity, which comprises administering a patient who is receiving cisplatin a therapeutically effective amount of an aldosterone blocker such as eplerenone or spironolactone.
US7041662 Substituted benzo [b] azepin-2-one compounds The invention relates to substituted benzo[b]azepin-2-one compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.
US20080318958 New utilities of tricyclic compounds Pharmaceutical compositions for enhancing the expression of apoAI are provided, which are used as medicaments for treatment of cardiovascular diseases on the basis of improving the functions of HDL. Pharmaceutical compositions for enhancing the expression of apoAI which comprises a compound of formula (I): in which X1 and X1 are independently an aryl or heteroaryl that may be optionally substituted, a hydrogen, a halogen, or the like; ring A is a benzene ring or 6-membered aromatic heterocyclic ring containing 1 to 3 N atoms that may be optionally condensed with another aromatic ring; R1 to R4 are independently a hydrogen, a halogen, a lower alkyl, a lower alkoxy or the like; a prodrug thereof, a pharmaceutically acceptable salt or solvate of them are disclosed.
EP1425281B1 Tricyclic CRF receptor antagonists The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof Please insert formula (I) here: to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
EP2390248A1 Flufenoxine derivatives for the treatment and prevention of amiloyd pathologies The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).
CN103263385A Celecoxib long-acting nano injection and preparation method thereof The invention relates to long-acting nano injection containing celecoxib serving as a main component and being used for treating rheumatoid arthritis and a preparation method of the long-acting nano injection. The celecoxib is slowly released in a human body through an intramuscular or subcutaneous injection method to reach a long-acting effect, and the effect can be kept for 3 days or longer. According to the preparation method, the long-acting nano injection of the celecoxib is prepared by combining airflow crushing and high pressure homogenization, the release degree and the bioavailability of the celecoxib are improved, and the effect of the celecoxib is prolonged at the same time. The celecoxib long-acting nano injection can be preserved in a prefilled syringe in a suspension form or preserved in a sealed container in a dry powder form. The injection in the prefilled syringe can be directly used for injecting, and the injection in the sealed container can be blended with a matched injection solution to form a suspension for injecting.
WO2011122916A3 Composition for increasing trail sensitivity, containing an inhibitor for inhibiting the expression or activity of tip41 which is a trail sensitizer target gene The present invention relates to a composition for increasing TRAIL sensitivity, which contains an inhibitor for inhibiting the expression or activity of the TIP41 protein. More particularly, it has been found that, when a hepatocellular carcinoma cell line which has TRAIL tolerance is treated with TIP41 siRNA and TRAIL, carcinoma-cell-specific apoptosis is induced, and apoptosis is induced not only in liver cancer but also in lung cancer and colorectal cancer which have TRAIL tolerance, and it has been found that, through animal experimentation, the size of a tumor is reduced and cancer cell apoptosis is induced, and the thus-induced apoptosis is caused by the activation of the MKK7/JNK delivery pathway due to the inhibition of TIP41 expression. Therefore, the composition containing the inhibitor for inhibiting the expression or activity of the TIP41 protein according to the present invention can be valuably used in the prevention and treatment of cancer or as anticancer adjuvants.
US20090061009 Composition and Method of Treatment of Bacterial Infections The invention is intended for a treatment of severe infections using an injectable drug-delivery system comprising nanoparticles of a biodegradable polymer with incorporated antibacterial drug.
WO2010028179A1 Heterocyclic compounds as gata modulators Novel heterocyclic compounds, stereoisomers thereof and/or pharmaceutically acceptable salts of formula (I) and its stereoisomers are provided. Additionally, methods of forming novel heterocyclic compounds, stereoisomers thereof and/or pharmaceutically acceptable salts of formula (I) and its stereoisomers are provided.
US20120302623 Novel Activation and Transfer Cascade for Ubiquitin A novel activating enzyme for ubiquitin, Uba6, is provided. Compositions and methods for inhibiting ubiquitin via the Uba6 pathway are provided. Methods of identifying novel inhibitors of ubiquitination are also provided. Novel RNAi molecules are also provided.
US7022328 Therapeutic and diagnostic compositions The present invention relates generally to therapeutic compositions for the treatment and/or prophylaxis of intestinal disease conditions in animals and birds caused or exacerbated by Lawsonia intracellularis or similar or otherwise related microorganism. The present invention also contemplates methods for the treatment and/or prophylaxis of such intestinal disease conditions and to diagnostic agents and procedures for detecting Lawsonia intracellularis or similar or otherwise related microorganism.
US8697680 Naphthoquinone derivatives useful for prevention of amyloid deposits and treatment of diseases involving amyloidogenesis The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.
US20050096312 Antiserotonine agents; antidepressants; eating disorders; anxiolytic agents; sleep disorders; gastrointestinal disorders; cardiovascular disorders; muscular disorders; endocrine system diseases; muscular disorders; psychological disorders Provided herein is a compound having the formula (I), (R2 is typically a tertiary nitrogen atom, being either alkyl-substituted or member of a heterocyclic ring; R7 is typically a monocyclic or bicyclic aromatic ring or a heterocyclic ring) wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.
US20120294869 Methods for Treating Fatty Liver Disease The present invention relates to the compositions, formulations and methods of treating fatty liver disorders, such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) and their sequelae by administration of uridine or a compound that modulates one or more uridine phosphorylases in a subject in need thereof.
WO2010149888A1 Derivatives of 2-mercaptocyclopentane carboxylic acid, method for the preparation thereof, and pharmaceutical compositions containing the same Compounds of formula (I) in which: R1 represents a hydrogen atom or a group of formula COR4, or else R1 represents a group of formula (A); R2 represents a group of formula NR5R6, or else R2 represents a nitrogen-containing heterocyclic, aryl or heteroaryl group; R3 represents a hydrogen atom or an alkyl group, m represents an integer between 1 and 6, n represents 0, 1 or 2, optical isomers thereof, and also the addition salts thereof with a pharmaceutically acceptable acid. Medicaments.
CN101367761A 6,7- substituted-2,2,4-trimethyl-tetrahydroquinoline-1-carboxylic acid aryl amide, synthesis and uses thereof The present invention relates to a 6, 7-substituted-2, 2, 4-trimethyl tetrahydro quinoline-1-carboxylic aryl amide compound, a preparation method thereof. The compound is used for preparing the medicine which can prevent cell procedural necrosis. And the compound has a structural formula as shown on the right, wherein, R1 is hydrogen, C1-4 linear chain alkyl or C1-4 alkoxyl; R2 is hydrogen or C1-4 linear chain alkyl; R3 is hydrogen, single substituted or double substituted C1-4 alkyl, C1-4 alkoxyl, halogen, acetyl or nitryl.
CN101255119A Novel tetrahydro curcumin derivatives and salt The invention belongs to medicine technic field, and relates to a series of novel tetrahydrocurcumin derivates which is tetrahydrocurcumin mannich base derivates and the salts thereof. The constitutional general formula of such compounds is represented by I, wherein RI represents alkyl group, or substituted or unsubstituted aralkyl; R2 represents: (1) hydrogen, (2) aliphatic secondary amido methane, (3) substituted or unsubstituted annular aliphatic secondary amido methen. The salts include hydrochloride, hydrobromate, Methanesulfonates and other pharmaceutical salts. The compounds of the invention has substantial pharmacological activity of anticancer, oxidation resistance, free radical remove and repressing activation of small cells.
WO2014136282A1 Crystalline form having specific crystal habit and pharmaceutical composition|containing this crystalline form as active ingredient Means for improving the solubility of luliconazole is provided. A crystal of luliconazole represented by the following formula is provided, wherein the crystal has such a crystal habit that (011) plane is a specific crystal growth plane. The crystal is characterized in that I(011) with respect to a sum total of I(001), I(100), I(10-1), I(011), I(110), I(11-1), I(10-2), I(11-2), I(020), I(021), I(20-2), I(121), I(013), I(11-3), and I(221) is not less than 25%, provided that integrated intensities of diffraction peaks, which correspond to the (001), (100), (10-1), (011), (110), (11-1), (10-2), (11-2), (020), (021), (20-2), (121), (013), (11-3), and (221) planes, are designated as I(001), I(100), I(10-1), I(011), I(110), I(11-1), I(10-2), I(11-2), I(020), I(021), I(20-2), I(121), I(013), I(11-3), and I(221) respectively in relation to the diffraction peaks detected in a range of 2θ= 5 to 35° in a powder X-ray diffractometry using CuKα radiation.
US7754228 Cytotoxic T-cell epitopes from Chlamydia Cytotoxic T-cell epitopes from C.pneumoniae proteins have been empirically determined. The epitopes from corresponding C.trachomatis proteins have also been identified, and some of these are identical to those from C.pneumoniae. The empirical method showed that algorithmic prediction was inadequate. The epitopes are useful for immunisation and/or diagnosis.
CN103304391A Biphenyl compound as well as preparation method and application thereof The invention discloses a biphenyl compound as well as a preparation method and an application thereof. The molecular formula of the biphenyl compound is C22H26O8, and the compound is named as neglignanD and has a structural formula shown in the specification. The preparation method comprises the following steps: performing extracting, organic solvent extracting, silicagel column chromatography, high performance liquid chromatography separation on the branches, leaves and fruit of dry schisandra chinensis which belong to macrophanerophytes and are used as raw materials. The application is the application of the biphenyl compound in preparing an anti-cancer drug. According to cytotoxic activity test, the neglignanD has good cytotoxic activity for cell strains such as NB4, A549, SHSY5Y, PC3 and MCF7. The compound disclosed by the invention is simple in structure, good in activity and good in application prospect and can be used as the pilot compound of the anti-cancer drug.
US20070293425 Mutein of a Bone Morphogenetic Protein and Use Thereof The present invention is related to a mutein of a bone morphogenetic protein, whereby the mutein comprises an amino acid substitution compared to the wildtype of the bone morphogenetic protein at the amino acid position corresponding to amino acid position 51 of human BMP-2.
WO2013178569A1 Pyrrolidino heterocycles The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
WO2011061271A1 Substituted carbamoylmethylamino acetic acid derivatives as novel nep inhibitors The present invention provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
CN103298795A Pure intermediate for preparing letrozole The present invention relates to an improved process for the preparation of Letrozole (I) and its synthetic intermediate 4-[(1-(1,2,4-triazolyl)methyl]benzonitrile (III). In particular, it relates to a process to prepare Letrozole and its intermediate (III) substantially free from regioisomeric impurities. The present invention further relates to acid addition salts of 4-[(1-(1,2,4-triazolyl)methyl]benzonitrile (III) such as the oxalate salt, and also to Letrozole (I), the intermediate (III) and salts thereof preparable by the processes of the present invention.
EP1542677A1 COMBINATIONS OF ATORVASTATIN AND a1, ADRENERGIC RECEPTOR ANTA GONISTS Combinations of atorvastatin and α1 adrenergic antagonists, the use of such combinations in the treatment of benign prostatic hyperplasia (BPH), methods of treating BPH using such combinations and medicaments containing such combinations are described.
US7943646 Benzamidine derivative, process for the preparation thereof and pharmaceutical composition comprising same The present invention relates to a novel benzamidine derivative, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The benzamidine derivative of the present invention effectively inhibits osteoclast differentiation at an extremely low concentration, and greatly increases the trabecular bone volume, and thus it can be advantageously used for the prevention and treatment of osteoporosis.
WO2006012422A1 Imidazopyrazine as tyrosine kinase inhibitors Compounds of the formula (I): and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF- 1 R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.
CN102697798A Application of adenosine in preparation of drug or food for preventing central nervous system oxygen toxicity (CNS-OT) The invention relates to application of adenosine in preparation of drug or food for preventing central nervous system oxygen toxicity (CNS-OT), belonging to the field of medicinal technology. Animal tests prove that adenosine can effectively prevent CNS-OT, so adenosine can be used in preparation of drug or food for preventing CNS-OT. The invention provides a new application of adenosine, and provides a new drug source for preventing CNS-OT.
US20100221330 Buoyant formulations of betaine An oral control release formulation for releasing at least one betaine after oral administration to a human, said formulation comprising at least one pharmaceutically acceptable means ensuring an at least partial floating of the formulation releasing at least one betaine in the gastro-intestinal tractus.
US7384919 Nontoxic; spray drying or freeze drying The inventors have devised novel approaches for the preparation of flavanolignan compositions of enhanced solubility and substantially free of toxic contaminants. Such novel approaches are based on spray drying or lyophilizing to dry a diluted preparation of flavanolignan. These approaches avoid the use of toxic excipients and or carriers commonly used to precipitate flavanolignan concentrates and thus address the drawbacks of existing methods and compositions.
CN102641353A Hair growth conditioner rich in plant flavonoids The invention discloses a hair growth conditioner rich in plant flavonoids, which is prepared by the following raw materials in ratio by weight: 30 to 90 of plant extract and 0.3 to 0.9 of synergist, wherein the plant extract is calculated on the basis of total flavonoids, the weight content of the total flavones is 10 to 50%, and the synergist is obtained by mixing niacinamide, vitamin B6, and zinc sulfate according to the weight ratio of 1 to 3:1 to 3:1 to 3. Compared with the prior art, the product provided by the invention utilizes a flavonoid compound in the plant extract to inhibit the generation of reductase leading to hair loss, and the synergist and the plant extract according to a special ratio have a synergistic effect, so that the active ingredient in the plant extract can better penetrate in stratum corneum and sebum of the hair skin and plays stronger hair growth, strengthening and blackening effects so as to further enhance the efficacies of loss prevention and hair growth promotion, and thus the hair loss can be prevented from the root.
US20120302608 Novel Imidazole Derivatives Useful for the Treatment of Arthritis The present invention provides compounds of the formula below: where A, X and R1-R6 are as described herein, a pharmaceutical salt thereof, and a pharmaceutical composition containing this compound; methods of treating pain associated with osteoarthritis using one of the compounds or a pharmaceutically acceptable salt thereof, and processes for preparing the compounds.
WO2009050159A1 Combination of fluticasone furoate with 4- [ (4-chl0r0phenyl)methyl] -2- ({ (2r)-i- [4-(4-{ [3-(hexahydr0-lh-azepin-l-yl) propyl ] oxy} phenyl) butyl] -2-pyrrolidinyl}methyl) -1 (2h) - phthalaz inone The present invention provides aqueous pharmaceutical compositions which comprise a compound which is 4-[(4-chlorophenyl)methyl]-2-({(2/R)-1-[4-(4-{[3-(hexahydro-1H-azepin- 1-yl)propyl]oxy}phenyl)butyl]-2-pyrrolidinyl}methyl)-1 (2H)-phthalazinone (I) or a pharmaceutically acceptable salt thereof, and to their use in the treatment of various inflammatory and/or allergic diseases such as allergic rhinitis.
US20080153888 Alpha-2-delta ligand/nsaid therapeutic treatment of lower urinary tract disorders The invention relates to a method of treating at least one symptom of lower urinary tract disease in a subject in need of treatment comprising administering to said subject a combination of an α2δ calcium channel subunit (A2d) ligand and a non-steroidal anti-inflammatory drug (NSAID), wherein the administered amounts of A2d ligand and NSAID together comprise a therapeutically effective amount of an active combination of agents. The combination of A2d ligand and NSAID can result in a synergistic therapeutic effect, wherein the combined effect is greater than the additive effect resulting from separate, single administration of A2d ligand or NSAID. Combination of A2d ligand and NSAID is particularly useful in treatment of lower urinary tract disease which manifests symptoms of urinary incontinence.
WO2010043631A1 Di-vanilloyl and tri-vanilloyl derivatives for use in anti-cancer therapy The invention relates to the medical field, more precisely in the field of anti-cancer treatment and treatment of Alzheimer's disease, Parkinson's disease or Pick's disease or for ameliorating symptoms of Down syndrome, providing newly synthesised multi-vanilloyl derivative compounds and their use in the treatment of said disorders.
US7501137 Process for controlling fecal hair excretion and trichobezoar formation A process and composition for controlling fecal hair excretion and trichobezoar formation in animals such as cats and rabbits is provided and includes feeding the animal a composition comprising from about 10 to about 42 wt % crude protein, from about 4 to about 30 wt % fat, from about 1 to about 25 wt % total dietary fiber, and a supplemental fiber source. The supplemental fiber source is present in amounts which provide from about 1 to about 13 weight percent of supplemental total dietary fiber. The animal is maintained on the diet for a sufficient period of time to control fecal hair excretion and trichobezoar formation.
EP2599489A1 AChE antisense deoxyoligonucleotide as an anti-inflammatory agent The present invention provides a novel use for AChE antisense oligonucleotides as anti-inflammatory agents, wherein said oligonucleotides are preferably as denoted by SEQ. ID. NO:1, SEQ. ID. NO:2 and SEQ. ID. NO:7. Described are pharmaceutical compositions for the treatment of inflammatory conditions comprising as active agent said AChE antisense oligonucleotides.
US20100069310 1-chloro-4-( beta -D-glucopyranos-1-yl)-2-[4-((1R,2R)-2-hydroxy-cyclopent-1-yloxy)-benzyl]-benzene; metabolic disorders such as diabetes, metabolic acidosis or ketosis, reactive hypoglycaemia, hyperinsulinaemia; sodium-dependent glucose cotransporter SGLT2 inhibitors Glucopyranosyl-substituted benzyl-benzonitrile derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
CN102190668A Quinazoline-2(1H)pyridinethione derivatives, and medicinal composition, preparation method and application thereof The invention relates to quinazoline-2(1H)pyridinethione derivatives shown as a general formula (I), and a preparation method and a medicinal composition thereof. The invention also discloses application of the quinazoline-2(1H)pyridinethione derivatives and the medicinal composition thereof in preparation of medicines for treating or preventing cancers and diseases related with cell apoptosis.
CN101390857A Medicine composition containing lansoprazole Disclosed is a lansoprazole medicine combination, which contains alkaline substance which is not less than 10% by weight and used as stabilizer. The lansoprazole medicine combination is used for the treatment of peptic ulcer.
WO2012171621A1 Pharmaceutical preparation for treating infections of the intestine with ehec bacteria The invention relates to a pharmaceutical preparation for treating infections of the intestine with EHEC bacteria, containing iodochlorohydroxyquinoline, and to a corresponding treatment.
CN102688243A Clathrate compound of perphenazine cyclodextrin derivative, and preparation method thereof The invention relates to a clathrate compound of a perphenazine cyclodextrin derivative, and a preparation method of the clathrate compound, aiming at solving the problems that perphenazine can not be dissolved in the water, and the medicine effect is low. The cyclodextrin derivative selected by the invention is hydroxypropyl-beta-cyclodextrin. The preparation method of the perphenazine hydroxypropyl-beta-cyclodextrin clathrate compound is simple in technology, easy to control, mild in clathration condition, short in production period and high in medicine content of the clathrate compound; and the clathrate compound can be mixed with pharmaceutic adjuvant to prepare any pharmaceutically acceptable oral administration preparation such as common tablets, orally disintegrating tablets, buccal tablets, etc.
US8110564 Bile acid or bile salt fatty acid conjugates The present invention relates to the use of a bile acid or bile salt fatty acid conjugate of general formula II W—X-G in which G is a bile acid or bile salt radical, which, if desired, is conjugated in position 24 with a suitable amino acid, W stands for one or two fatty acid radicals having 14-22 carbon atoms and X stands for a suitable bonding member or for a direct C═C bond between said bile acid or bile salt radical and the fatty acid(s) or of a pharmaceutical composition comprising same for the reduction of Cholesterol in blood, for the treatment of Fatty Liver, Hyperglycemia and Diabetes.
US20120178799 Energy beverage with creatine and caffeine combination The present invention is an energy drink that included both creatine and caffeine, which provides superior energy, concentration and performance over other energy beverages/liquids. The invention can include other vitamins and beneficial additives, but is intended to be unflavored and unsweetened.
WO2010149363A3 Pharmaceutical composition comprising rotigotine salts (acid or na), especially for iontophoresis The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1- ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fybromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
US7019014 Process for producing anticancer agent LL-D45042 The disclosure describes the production of anticancer agent LL-D45042, having the structure: by fermentation, to methods for the recovery and concentration of this anticancer agent from crude solutions, and to processes for the purification of this anticancer agent as well as a new microorganism of the species Streptomyces hygroscopicus LL-D45042 and mutants thereof useful in the preparation of this compound.
EP2781219A1 Use of sedoheptulose for prevention or treatment of inflammation The invention discloses sedoheptulose for use in the prevention or treatment of inflammation.
WO2010145206A1 Preparation methods of optical isomers of stepholidine or its derivatives and intermediates thereof Preparation methods of optical isomers of stepholidine or its derivatives and intermediates thereof are disclosed. Especially, Preparation methods of L-stepholidine or optical isomers of its derivatives are disclosed. Said optical isomers of stepholidine or its derivatives are prepared by catalytic asymmetric hydrogenation from 3,4-dihydroisoquinoline of formula I in the participation of the chiral metal catalyst.
US20120041055 Composite polynucleic acid therapeutics Compositions comprising therapeutic polynucleic acids and method of use. The compositions comprise one or more polynucleic acid sequences having two or more features useful for treating diseases associated with cellular proliferation or growth.
CN1586496A Baicalin soft capsule and its preparing method The present invention relates to soft baicalin capsule and its preparation process. The present invention includes active component, solvent, diluent, emulsifying co-solvent and antioxidant stabilizer. It includes baicalin as active component in 30-80 wt%, preferably 40-60 wt%; solvent and diluent in 25-60 wt%, preferably 35-50 wt%; emuilsifier for raising the dissolubility of baicalin in animal and plant oil and raising the stability of baicalin in 3-10 wt%, preferably 4.5-8.5 wt%; antioxidant stabilizer to raise the antioxidant performance of the product in 1-3 wt%, preferably 1.5-2.5 wt%. The soft capsule shell is prepared with gelatin, glycerin, sorbic alcohol, etc. and has titania in 0.2-1.2 wt%, preferably 0.5-0.7 wt%, of gelatin added as light screening agent.
EP1898906A2 Methods of treatment utilizing certain melatonin derivatives A method for treating anxiety disorders, affective disorders, obesity, intracranial injury, spinal cord injury, neurodegenerative diseases, sclerosis, migraine, fibromyalgia and cerebrovascular disease, using melatonin derivatives is disclosed. A specific melatonin derivative for use in the disclosed process is β-methyl-6-chloromelatonin (otherwise referred to as (R) -N- [2- (S-chloro-B-methoxy-lH-indol-S-yl) propyl] acetamide) .
US20100111944 Method of diagnosing, classifying and treating endometrial cancer and precancer Diagnostic and therapeutic applications for endometrial cancer are described. The diagnostic and therapeutic applications are based on certain activation mutations in the FGFR2 gene and its expression products. The present invention is directed to nucleotide sequences, amino acid sequences, probes, and primers related to FGFR2 activation mutants and kits comprising these mutants to diagnosis and classify endometrial cancer in a subject.
WO2012094834A1 Compound traditional chinese medicine extract for prevention and treatment of glycometabolism disorders and preparation method thereof The compound traditional Chinese medicine extract for the prevention and treatment of glycometabolism disorders, wherein the active ingredients of the extract are composed of 1-cerotol, β-sitosterol, n-hexacosanoic acid, atractylenolide III, oleanolic acid, berberine, jateorrhizine, coptisine, tanshinol, salvianolic acid B, cyclotetracosane, 9,12-octadecadienoic acid, 5,7-dimethoxycoumarin, specnuezhenide, ginsenoside Rb1 and Rg1, notoginsenoside R1 and eucommiol. The preparative method comprises extracting crude drug Radix Salviae Miltiorrhizae, Fructus Ligustri Lucidi, Rhizoma Coptidis, Herba Cirsii Japonici, Cortex Eucommiae, Rhizoma Atractylodis Macrocephalae, Radix Notoginseng and Fructus Citri Sarcodactylis with C1-3 alcohol and/or water, combining total extracts, extracting the total extracts with different organic solvents (such as petroleum ether, ethyl acetate and n-butyl alcohol) to obtain effective part separately, and blending every effective part to obtain the product.
WO2009144392A1 Polysubstituted derivatives of 6-heteroaryl-imidazo[l,2- α] pyridines, and preparation and therapeutic use thereof Compounds of Formula (I) (I), wherein: R1 is a phenyl or naphthyl group, a heteroaryl group, or a heterocyclic group, optionally substituted for one or a plurality of atoms or groups; Het is a monocyclic heteroaryl group comprising 5 to 6 atoms, 1 to 3 heteroatoms of which are selected from N, O, and S; X is 1 to 3 substituents, identical to or different from each other and selected from hydrogen, halogen, (C1-C10)alkyl, (C1-C10)alcoxy, NRaRb, nitro, or cyano, the (C1-C10)alkyl capable of being substituted for one or a plurality of groups selected from halogen,(C1-C10)alcoxy, (C1-C10)haloalcoxy, NRaRb, or hydroxyl; R, in positions 3, 5, 7, or 8 of rimidazo[1,2-α]pyridine, is 1 to 4 substituents, identical to or different from each other and selected from hydrogen, halogen, (C1-C10)alkyl, halo(C1-C10)alkyl, or (C1-C10)alcoxy; R2 and R3, independently of each other, represent a hydrogen atom or a (C1-C10)alkyl group, this group being optionally substituted for an Rf group; an aryl group optionally substituted as a base or salt having an acid added. The invention is used in therapy and in synthesis methods.
US7803807 such as trans-2-[3'-oxospiro [cyclohexane- 1,1'(3'H)-isobenzofuran]-4yl]-5-(2-pyridyl) imidazo[4,5-b]pyridine, exhibiting neuropeptide Y antagonistic effects, used for the treatment of cardiovascular, nervous system, metabolic, gastrointestinal, sexual and respiratory system disorders; pharmacokinetics The present invention relates to compounds of Formula (I) wherein A, B and C are independently methine, said methine being optionally substituted; D is nitrogen; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted and least two of T, U, V and W are said methine groups; X is —N(SO2R4)—, N(COR5)— or —CO—; Y is C(R6)(R7)—, —O— or —N(R8) and a pharmaceutically acceptable salt, ester or N-oxide derivative thereof.
WO2014113607A1 Protective molecules against anthrax toxin Disclosed herein inter alia are compositions and methods useful in the treatment of infectious diseases and exposure to toxins.
CN103083313A Application of substituted pyrrole chromones compound in preparation of drug for treating diseases related to 5 type phosphodiesterase The invention relates to an application of substituted pyrrole chromones compound in preparation of a drug for treating diseases related to 5 type phosphodiesterase. The substituted pyrrole chromones compound has a structure shown in the specification, wherein R1, R2, R3 and R4 are selected from hydrogen, halogen, C1-3 alkyl, C1-3 substituted alkyl, alkoxy, acyl, carboxyl, carboxylate radical, nitrogen-containing group, phosphorus-containing group or sulfur-containing group; R5 is selected from halogen, C1-3 alkyl, C1-3 substituted alkyl, alkoxy, acyl, carboxyl, carboxylate radical, nitrogen-containing group, phosphorus-containing group, sulfur-containing group, aromatic group and amino acid side chain structure; R6 is selected from hydrogen or C1-3 alkyl, acyl, carboxyl-containing group, carboxylate radical-containing group, nitrogen-containing group, phosphorus-containing group or sulfur-containing group; and X is selected from substituted or non-substituted cyclic group. The compound can be used for preparation of the drug for treating diseases related to 5 type phosphodiesterase, and is particularly suitable for preparation of the drug for treating male sexual dysfunction or pulmonary hypertension disease.
CN102743333A Levetiracetam oral liquid and preparation method of levetiracetam oral liquid The invention belongs to the technical field of medicines and particularly provides a levetiracetam oral liquid and a preparation method of the levetiracetam oral liquid. The levetiracetam oral liquid is prepared by the step of mixing levetiracetam with one or more of sweeteners, buffer agent, a preservative, a solvent and a flavouring agent. The levetiracetam oral liquid can effectively improve the life quality of patients with epileptic diseases and improves the medicine compliance of the patients.
US7229987 Oxazoles with one or more tertiary amine groups and phenyl groups, e.g., 1-{4-[2-(Benzofuran-2-ylmethoxymethyl)-oxazol-5-yl]-phenyl}-3-(2-dimethylamino-ethyl)-urea and -(3-{4-[2-(2-Phenoxy-ethylsulfanylmethyl)-oxazol-5-yl]-phenoxy}-propyl)-azepine; treating obesity and related diseases, e.g., diabetes The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
EP2736519A1 Alkaline compositions and their dental and medical use The present invention relates to antimicrobial alkaline compositions suitable for use in medical and dental treatment. The compositions comprise a polyalkylene glycol or C3-C6 polyol compound and calcium hydroxide or components that generate calcium hydroxide in situ. The use of the compositions as dental medicaments, obturants, liners, oral disinfectants and bone cements is also described.
WO2013171252A1 Means to facilitate food intake and food retention The invention provides for means for a method to facilitate food intake and food retention in a mammal by applying a sufficient dose of a local anesthetic drug in the lumen of the pharyngeal-esophageal-gastric-duodenal tract before or during or after eating. The local anesthetic can be amethocaine, articaine, benzocaine, bupivacaine, chloroprocaine, cinchocaine, cyclomethycaine, dibucaine, diethocaine, etidocaine, larocaine, levobupivacaine, lidocaine, lignocaine, mepivacaine, novocaine, piperocaine, prilocaine, procaine, proparacaine, propoxycaine, QX-222, QX-314, ropivacaine, tetracaine, trimecaine, menthol, eugenol or a safe pharmaceutical formulations of tetrodotoxin, saxitoxin, or neosaxitoxin. The invention is useful for patients having problems with food intake or food retention.
WO2009120801A3 Ikki inhibitor therapies and screening methods, and related ikki diagnostics The present invention provides diagnostics, screening methods, and treatment methods related to obesity, insulin resistance, diabetes, weight loss, and related disorders. In particular, the present invention provides methods of treating such conditions with IKKi inhibitors, methods of diagnosing such conditions based on IKKi status, and methods of screening candidate IKKi inhibitors.
CN102357086A Cefprozil orally disintegrating tablets The invention belongs to the field of medicinal preparations, in particular to cefprozil orally disintegrating tablets. Cefprozil is coated with powder, and, together with proper disintegrating agent, flavoring agent, filling agent and the like, is prepared into the cefprozil orally disintegrating tablets. The orally disintegrating tablets are portable, and convenient to take, have good mouthfeel, ensure that a medicine is quickly dissolved out, and have quick response.
US7622612 Tricyclic derivatives and their use The present invention relates to tricyclic colchicine derivatives represented by the formulas (I) or (II), pharmaceutically acceptable salts thereof, and a method for providing an immuno-suppressive or immuno-modulating effect, an anti-proliferative effect, an anti-inflammatory effect or a method for treating cancer comprising administering to a patient an effective amount of one or more colchicine derivatives:
US20100286285 Pharmaceutical composition comprising oleaginous ointments and vitamin D or its derivatives in the solubilized state The present invention relates to an anhydrous pharmaceutical composition for use in the treatment of psoriasis and other skin disorders, characterized in that it comprises an oleaginous ointment and, as active ingredient, a compound chosen from vitamin D and its derivatives, said active agent being in a solubilized form in said composition.
WO2006075748A1 Therapeutic agent for allergic conjunctival disease Novel pharmacological efficacy (pharmaceutical usage) of 9-cyclopentyl-7-ethyl-3-(thiophen-2-yl)-5,6-dihydro-9H-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-a]pyridine and 2-(3-chlorophenoxy)-3-[3-(3-hydroxypyridin-4-yl)propoxy]pyridine. These substituted pyridine derivatives without exception exhibit excellent allergic conjunctival symptom suppressing effects on allergic conjunctival models, so that they are useful as a therapeutic agent for allergic conjunctival diseases, such as allergic conjunctivitis, spring catarrh and atopic keratoconjunctivitis.
US20120157405 Methods and Compositions for the Treatment of "Burning Feet Syndrome" A composition for the treatment of “Burning Feet Syndrome” includes pantothenic acid or its analogs, or its derivatives, or its synonyms, alpha-lipoic acid or its analogs, or its derivatives, or its synonyms, and L-arginine or its analogs, or its derivatives, or its synonyms. The composition may also include at least one substance selected from the group consisting of B1, B2, B3, B6, B7, B9, B12, Acetly-L-Carnitine, N-acetlycystein, Omega-3 fatty acids, Omega-6 fatty acids, Vitamin E, and Taurine or any of their analogs, derivatives, or synonyms. The composition is used in a method for the treating of “Burning Feet Syndrome” by administering to a human such a composition.
CA2808237A1 High dose buprenorphine compositions and use as analgesic The present disclosure relates to a method of providing prolonged analgesia to a mammal in need thereof. Specifically, the current disclosure is directed to a method of treating pain in a mammal for a prolonged period of time using a single high dose of a buprenorphine formulation.
CN103127434A Pharmaceutical composition for treating bone trauma The invention discloses a pharmaceutical composition for treating a bone trauma. The pharmaceutical composition for treating the bone trauma is composed of psammosilene tunicoides, euphorbia pekinensis, dendrobium nobile, rhizoma drynariae, white radix achyranthis bidentatae, sambucus williamsii, lycopodium clavatum, sappanwood, cudrania cochinchinensis kudo et masam, musk, tortoise plastron, brasenia peltata tursh, ground beeltle, cornu bubali, yam rhizome, rhizoma kaempferiae, artemisia anomala and calcined natural copper. Conventional auxiliary materials are added into the pharmaceutical composition according to a conventional process, so that clinic acceptant emplastrum or spray or ointment or liniment or tinctures is made. The pharmaceutical composition for treating the bone trauma has the effects of being capable of achieving reunion of bone, muscle and ligament, warming and activating meridian, activating blood and dissolving stasis, and relieving swelling and pain, has good treatment effects for treating bone traumas such as injury of tendon and muscle and fracture, traumatic injury and stagnant blood coagulation, and has no toxic and side effects.
CN102670569A Method for preparing absorbable minocyline drug diaphragm The invention relates to a method for preparing an absorbable minocyline drug diaphragm, which comprises the step of operating that 1 hydrochloric acid minocyline powder is dissolved into distilled water to obtain hydrochloric acid minocyline solution; 2 gelatin is added into the hydrochloric acid minocyline solution in water bath at 40 DEG C to be uniformly mechanically stirred away from light; 3 glycerin is further added in the water bath at 40 DEG C to go on to be uniformly stirred and obtain faint yellow viscous liquid; 4 the faint yellow viscous liquid is paved on a plate to be made into a diaphragm in room temperature, and a gel diaphragm which has a thickness of 0.5-0.6mm is obtained after solidifying; and 5 the gel diaphragm is frozen and dried to obtain the absorbable minocyline drug diaphragm. The method for preparing the absorbable minocyline drug diaphragm is simple in operation, excellent in controlling, environmental friendly and high in yield. The method for preparing the absorbable minocyline drug diaphragm is convenient to be applied in clinical, compared with similar products abroad, the absorbable minocyline drug diaphragm has excellent cost performance, and does not have obvious difference in effects of clinical application.
WO2009049410A1 Clioquinol for the treatment of hematological malignancies The present invention relates to compositions and methods for treating hematological malignancies and proliferative diseases, disorders and conditions involving increased D-cyclin expression. In particular, the present invention relates to compositions and methods for treating the hematological malignancies acute myeloid leukemia (AML) and multiple myeloma (MM) using clioquinol.
EP2683369A1 Multiantivirus compound, composition and method for treatment of virus diseases A method for obtaining a new antiviral compound with multiple action against many viruses, comprising modified highly purified yeast RNA, a pharmaceutical composition comprising such RNA, and a method for the treatment and prevention of viral disease comprising administering to a patient a composition comprising an amount effective to ameliorate the symptoms of viral disease of ribonucleic acid. The exogenous modified yeast RNA has a pronounced multiple anti-virus action in a wide range of concentrations. The modified yeast RNA is capable of inhibiting the reproduction of viruses from Orthomyxoviridae, Paramyxovirus, Hepatitis, Herpesviridae families, enterovirus and adenovirus. Also, the modified yeast RNA is capable of inhibiting the reproduction of influenza viruses, hepatitis C virus, genital herpes, human immunodeficiency virus and Coxsackie B virus.
US7446103 N-[4-(3-Piperidin-1-ylpropoxy)-benzoyl]-5-fluoroisoindoline; Alzheimer's disease; cognition enhancers; amidation The present invention relates to novel bicyclic benzamide derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
EP1534274A1 Combination of an allosteric alkyne inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib The invention provides a combination, comprising an allosteric alkyne inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with celecoxib, or a pharmaceutically acceptable salt thereof, or valdecoxib, or a pharmaceutically acceptable salt thereof. This invention also provides a method of treating a disease that is responsive to inhibition of MMP-13 and cyclooxygenase-2, comprising administering to a patient suffering from such a disease the invention combination comprising an allosteric alkyne inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with celecoxib, or a pharmaceutically acceptable salt thereof, or valdecoxib, or a pharmaceutically acceptable salt thereof. This invention also provides a pharmaceutical composition, comprising the invention combination comprising an allosteric alkyne inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with celecoxib, or a harmaceutically acceptable salt thereof, or valdecoxib, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. The invention combinations may also be further combined with other pharmaceutical agents depending on the disease being treated.
CN101703536A Antitumor medicament with combination of spirulina polysaccharide and ginkgo-leaf effective components The invention provides an antitumor medicament with combination of spirulina polysaccharide and ginkgo-leaf effective components, which relates to an antitumor medicament. The antitumor medicament is formed by combining spirulina polysaccharide and ginkgo-leaf effective components, wherein the mass ratio of the spirulina polysaccharide to the ginkgo-leaf effective components is 0.35-1.5:0.35-1.5; the optimal mass ratio of the spirulina polysaccharide to the ginkgo-leaf effective components is 1:1; the spirulina polysaccharide is a water-soluble complex heteropolysaccharide, has the polysaccharide content more than or equal to 93 percent, is formed mainly by connecting D-mannose, D-glucose, D-galactose and glucuronic acid through alpha-type glycosidic bonds, and has the molecular weight of about 12,590 D; and the ginkgo-leaf effective components have the total-flavonoid content more than or equal to 24 percent and the terpene-lactones content more than or equal to 6 percent. The medicament has remarkable tumor-inhibiting effect on S180 sarcoma growing in vivo, as well as human colon cancer HT29 cells, human leukemia HL60 cells, human gastric cancer MGC cells, human cervical carcinoma HeLa cells, human hepatoma 7402 cells and human breast cancer cells growing in vitro.
CN103239419A Method for preparing theophylline sustained release The invention belongs to the technical field of medicines and relates to a method for preparing theophylline sustained release. The method comprises the following preparation steps: (1) adding a retardant into a wet type granulator, adding a solvent of the retardant to prepare an adhesive, and stirring and shearing at normal temperature; (2) adding theophylline, an adhesive and a filler and preparing a soft material; (3) replacing a 16-20-mesh stainless steel mesh in the granulator, and granulating through the granulator; and (4) pumping the wet granules into a fluidized bed for drying in a vacuum mode, granulating through a crushing granulator, mixing and laminating to obtain the theophylline sustained release by adding a lubricating agent. The theophylline sustained release can be released at a constant speed, the quality is stable, the pain of the asthmatic is safely, effectively and stably solved, the pain of a patient is relieved, the process is simple, and the process stability is high.
WO2010078542A1 Three layer tablet containing cetirizine, pseudoephedrine, and naproxen In one aspect, the present invention features a tablet including a first drug layer, a second drug layer, and a third drug layer, wherein (i) the first drug layer includes naproxen; (ii) a second drug layer including pseudoephedrine; and (iii) the third drug layer includes cetirizine; wherein the first drug layer is in contact with the second drug layer, the third drug layer is in contact with the second drug layer, and the first drug layer is not in contact with the third drug layer, and wherein the second drug layer is a sustained release layer adapted to deliver a therapeutically effective amount of pseudoephedrine for a period of at least twelve hours.
CN103156106A Lipid lowering and liver protecting drug or health food prepared by active ingredients of fructus schisandrae chinensis and preparation method The invention discloses a lipid lowering and liver protecting drug or health food and a preparation method. The lipid lowering and liver protecting drug or health food is prepared by active ingredients of fructus schisandrae chinensis in particular to fructus schisandrae chinensis polysaccharide. The fructus schisandrae chinensis polysaccharide can be prepared to accessible dosage forms such as troches, capsules, granules, pills, oral liquid and the like. The lipid lowering and liver protecting drug or health food has good lipid lowering and liver protecting effects, can serve as food and a drug, is without toxic side effects, is suitable for prevention and treatment of a hyperlipidemia disease and a fatty liver disease, uses general-purpose equipment, is beneficial for industrialized mass production, and chosen materials are easy to get.
US20100179095 Use of folates for producing a preparation suitable for preventing and treating inflammation and diseases associated with inflammation, especially for influencing the inflammation markers crp and saa This invention relates to the use of folates for producing a pharmaceutical preparation suitable for the prevention and treatment of inflammation and of diseases associated with inflammation, particularly for influencing the inflammation markers C-reactive protein (CRP) and serum amyloid A protein (SAA). The clinical areas of application are all anomalies of the CRP and SAA levels. The invention also relates to pharmaceutical preparations for the prevention and treatment of inflammation and of diseases associated with inflammation, particularly for influencing CRP and SAA levels, characterised in that as an active ingredient it comprises at least one compound which is selected from the group consisting of pteroic acid monoglutamate (folic acid), dihydrofolic acid, 5-formyltetrahydrofolic acid, 5-methyltetrahydrofolic acid, 5,10-methylenetetrahydrofolic acid, 5,10-methenyl-tetrahydrofolic acid, 10-formyltetrahydrofolic acid or tetrahydrofolic acid, polyglutamates thereof, optical isomers thereof, particularly optically pure natural isomers thereof, and mixtures of optical isomers also, particularly racemic mixtures, as well as pharmaceutically acceptable salts thereof also, together with pharmaceutically acceptable active ingredients and adjuvants.
WO2011002161A2 Transdermal composition comprising tolterodine A transdermal composition comprising tolterodine having improved storage stability is disclosed. The transdermal composition comprising tolterodine contains an antioxidant to stabilize tolterodine and can be stored for a long period of time.
US20090030077 Novel Fenofibrate Formulations and Related Methods of Treatment The invention provides novel omega-3 oil liquid formulations of fenofibrate. These formulations can be substantially free of any food effect, effective in small volumes, and readily bioavailable. Notably, because the formulations of the invention contain an omega-3 oil as the major ingredient, they not only provide anithypercholesterolemic and antihypertriglyceridemic effects due to the fenofibrate active ingredient, they also provide recommended daily dosages of omega-3 oils (i.e., approximately 1 gram of omega-3 oil per day), or a portion thereof.
US20120225901 Dosage form containing oxycodone and naloxone The present invention concerns a dosage form comprising oxycodone and naloxone which is characterized by specific in vivo parameters such as tmax, Cmax, AUCt value, mean bowel function score and/or duration of analgesic efficacy.
EP1194425B1 Substituted benzimidazole The invention relates to compounds of formula (I) which are suitable for producing medicaments. Said medicaments are used in the prophylaxis and treatment of diseases, in the course of which there is increased activity of NFkB.
CN103550248A Bacterial cellulose/ chitosan composite film spraying agent and preparation method thereof The invention relates to a bacterial cellulose/ chitosan composite film spraying agent and a preparation method thereof. The composite film spraying agent comprises bacterial cellulose, chitosan and a common solvent of bacterial cellulose and chitosan. The preparation method comprises the following steps of crushing and drying bacterial cellulose and chitosan; adding an NMMO (N Methyl Morpholine Oxide) aqueous solution; premixing to obtain a slurry mixture suspension without being dissolved completely; performing reduced pressure distillation to reduce the moisture content of the solvent to be 13 to 15%, thus obtaining a solution with the sum of mass concentration of bacterial cellulose and chitosan of 2 to 4%; uniformly agitating; standing; and finally filtering and defoaming. The bacterial cellulose/chitosan composite film spraying agent is high in tensile strength, water binding capacity and air and water permeability, and high in shape maintaining capacity, overcomes the shortcomings of inconvenient use and non-ideal curative effect of powdered or paste type film spraying agents, and also overcomes the shortcomings that of the film formed by a pure chitosan film spraying agent in a wounded part is low in strength, easy to deform and limited in liquid absorbing ability.
EP1432669B1 4-(c2-6 alkoxy)-substituted chalcones as therapeutic agents The present invention pertains to compounds of the following formula: (1) wherein: RALK is primary or secondary aliphatic saturated C2-6alkyl; each of RB2, RB3, RB4, and RB5 is independently -H, -OH, or -OMe; each of R1 and R2 is independently: -H, optionally substituted C1-4alkyl, or optionally substituted C5-20aryl; RA3 is -H, -OH, -OC(=O)RE, -OS(=O)2OH, or -OP(=O)(OH)2; RE is : -H, optionally substituted C1-6alkyl, optionally substituted C3-20heterocyclyl, or optionally substituted C5-20aryl; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.
WO2014085528A1 Azaquinazoline carboxamide derivatives Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.
EP1196427B1 C-19-halogen-substituted steroids of the androst-9(11)-ene-series, methods for the production and use thereof The invention relates to novel C-19-halogen-substituted steroids of the androst-9(11)-ene series, i.e. 17β-hydroxy-19-halogen-androsta-4,9(11)-diene-3-one of general formula (I) and to methods for the production thereof. The invention also relates to the use of novel radiohalogen-marked compounds of formula 1 as radiopharmaceuticals. The invention further relates to non-marked compounds(I) of formula I as initial products for the production of novel biologically effective 5β-substituted Androst-9(11)-enes of general formula (II) and novel 6β 19-cycloandrostadienes of formula (III), in addition to methods and uses thereof.
US6974568 Treatment for cough The invention discloses the existence of cannabinoid receptors in the airways, which are functionally linked to inhibition of cough. Locally acting cannabinoid agents can be administered to the airways of a subject to ameliorate cough, without causing the psychoactive effects characteristic of systemically administered cannabinoids. In addition, locally or systemically administered cannabinoid inactivation inhibitors can also be used to ameliorate cough. The present invention also defines conditions under which cannabinoid agents can be administered to produce anti-tussive effects devoid of bronchial constriction.
EP1039911B1 MORPHOLINO-N-ETHYL ESTER PRODRUGS OF INDOLE sPLA 2 INHIBITORS The compound, ((3-(2-amino-1,2-dioxoethyl)-1-((1,1'-biphenyl)-3-ylmethyl)-2-methyl-1H-indol-4-yl)oxy)acetic acid morpholino-N-ethyl ester, is disclosed together with its use as a highly bioavailable indole compound for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.
EP1253924B1 Nitrate salts of antimicrobial agents Nitrate salts of antimicrobial agents for the preparation of antimicrobial medicaments, specifically antiviral, antifungal and antibacterial medicaments.
CA2418167C Compositions and methods of preventing or reducing the risk or incidence of skeletal injuries in horses The present invention relates to compositions and methods of preventing or reducing the risk or incidence of skeletal injuries in horses. The present invention further relates to compositions and methods for alleviating pain associated with skeletal injuries in horses and to treating skeletal injuries in horses.
CN1561998A Anti-platelet medicine and its use An anticoagulant medicine for preventing and treating arterial thrombosis contains heraclenin, and pharmacologic carrier and/or excipient.
WO2013154503A1 Methods for bladder cancer therapy using baculoviral vectors There is presently provided methods and uses relating to delivering a nucleic acid molecule to a bladder cell using a baculoviral vector. The bladder cell is contacted with a baculoviral vector, which may further comprise a transgene.
CN102614204A New application of stilbene glucoside to hangover alleviation The invention provides new application of stilbene glucoside to hangover alleviation. The stilbene glucoside has the functions of alleviating hangover and protecting liver, and inducing resuscitation and benefiting intelligence, and has the effect of preventing and treating alcoholic liver, fatty liver, liver injury, cerebral injury, memory deterioration and the like which are all caused by long term or quantity of alcohol drinking. The stilbene glucoside can be applied to hangover-alleviating medicaments. The stilbene glucoside and pharmaceutically acceptable salts, esters or sugars thereof are used for preparing the hangover-alleviating medicaments. The stilbene glucoside and the pharmaceutically acceptable salts, esters or sugars thereof can be prepared into pharmaceutically acceptable formulations, such as tablets, capsules, solutions, injections, granules, drips, micro pills and the like. The stilbene glucoside has wide application prospect in aspects of medical healthcare and the like.
CN101524359A Medicament for treating penis erectile dysfunction The invention discloses a medicament for treating penis erectile dysfunction, which is characterized in that effective components of the medicament comprise hyperin and/or hypericin. Pharmacological experiments and clinical experiments show that the medicament has the advantages of small side effects, wide therapeutic window and the like, and the medicament does not generate consequential effects on patients after taking and has the characteristics of natural medicaments; besides, the medicament has good pharmacological effects.
WO2013089307A1 Composition for inhibiting after-cataract and method for preparing same The present invention relates to a composition for inhibiting after-cataract comprising hydrophilic sulfasalazine, a high content of hyaluronic acid, and a carrier comprising an acqueous solution, and a method for preparing the composition for inhibiting after-cataract by adding a hyaluronic acid powder to sulfasalazine that is hydrophillized, and mixing same according to specific reaction conditions.
WO2013110280A1 Panobinostat for use in the treatment of hiv-1 The present invention relates to uses and methods involving Panobinostat and HIV-1. In particular relates the present invention to Panobinostat for use in the treatment of HIV-1 and especially latent HIV-1. This is done using a low dosage of Panobinostat which is highly effective in depleting the HIV-1 reservoir.
US20060009416 Vitamin B6, pyridinoline, 3-hydroxypyridine, or an N-alkyl-3-hydroxypyridine; sunscreen agents The invention relates to methods for modulating photodamage via the use of collagen derived molecules which either enhance or inhibit damage caused by ultraviolet light.
CN101511857A 18-methyl-19-nor-androst-4-en-17,17-spiroether (18-methyl-19-nor-20- spirox-4-en-3-one) and pharmaceutical preparations containing the same The invention relates to novel 18-methyl-19-nor-androst-4-en-17,17- spiroether of general formula (I), where Z = O, two H, =NOR or =NNHSO2R, R = H, or straight or branched chain C1-4 or C3-4alkyl, R = H, halogen, or CF3 and R and/or R are a- or ss-positioned and R and R independently = H or straight or branched chain C1-4 or C3-4alkyl or a straight or branched chain C2-4 or C3-4alkylene or a saturated C3-5 cycloalkyl, or together form a methylene group or a double bond. The novel compounds have gestagenic and antimineralcorticoid action.
EP2352722A2 Hydroxyadamantyl inhibitors of dipeptidylpeptidase iv The present invention relates to new hydroxyadamantyl inhibitors of dipeptidylpeptidase IV activity, pharmaceutical compositions thereof, and methods of use thereof. Formula (I).
WO2013051330A1 Treatment of atrial fibrillation by means of vidarabine Provided is a novel antiarrhythmic agent. An antiarrhythmic agent containing vidarabine, and a pharmaceutically accepted salt or solvate thereof.
WO2005121129A1 Novel propenone derivatives containing aromatic rings, a maufacturing process thereof and a composition containing the same using as an antiinflammatory agent The present invention is related to novel propenone derivatives containing aromatic ring, a manufacturing process thereof and a composition containing the same using as an anti¬ inflammatory agent. The compound of the present invention show potent anti-inflammatory activity confirmed by various experiments for example, the inhibition test of COX and 5-LOX enzyme activity, the inhibition test of LTC reproduction and NO production, MTT assay test, the inhibition test on the iNOS and COX-2 protein expression and PGE reproduction using RAW 264.7 macrophage etc. Accordingly, present compounds can be useful in treating and preventing various inflammatory.
US20100234347 Substituted Pteridines substituted with a Four-Membered Heterocycle The invention relates to novel pteridines of formula (1), suitable for the treatment of airway or gastrointestinal complaints or diseases, inflammatory diseases of the joints, the skin or eyes, diseases of the peripheral or central nervous systems or cancerous diseases and pharmaceutical compositions comprising said compounds.
CN101568342A Treatment for multiple myeloma The present invention provides methods of treating a subject suffering from multiple myeloma comprising administering to the subject an effect amount of a compound according to Formula I.
EP2310005A2 Treatment of inflammatory conditions with isothiocyanates The present invention concerns compositions that may be used in the prevention or treatment of medical conditions characterised by having an inflammatory component. The compositions comprise a therapeutically effective amount of an isothiocyanate (ITC). The composition may comprise further anti-inflammatory agents (e.g. plant- derived polyphenols).
CN1739569A Dietotherapeutic nutrient for preventing and treating non-insulin independent diabetes and its prepn process The dietotherapeutic nutrient for preventing and treating non-insulin independent diabetes consists of purine nucleotide, compound vitamin, compound trace elements, compound mineral matter, essential fatty acid oil and proper amount of edible cellulose as stuffing and hypoglycemic. The dietotherapeutic nutrient is used as main material or additive for food products and medicines for preventing and treating diabetes through balancing insulin and hyperglycemic hormone, repairing the functions of pancreatic island and kidney, preventing and treating complication and restoring normal synthesis and metabolism. The present invention has c-GMP, trace elements, etc. to regulate second messenger c-AMP amount, lift, activity and release time of hyperglycemic hormone, calcium carbonate to buffer and neutralize flavone and other acid matter and acid poisoning, potassium citrate to replenish potassium and to maintain acid-alkali and electrolyte balance. The dietotherapeutic nutrient has no toxic side effect and dependence.
US7053117 Substituted 4H-chromenes and analogs as activators of caspases and inducers of apoptosis and the use thereof The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the general Formula I: wherein R1–R5, A, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
US20100222438 Methods compositions and article of manufacture for modulating bone growth Novel methods and pharmaceutical compositions suitable for modulating bone growth and remodeling, preventing bone diseases, inducing bone growth or repair by cannabinoid receptor-mediated effects on bone cells is disclosed. Methods of identifying bone growth modulating agents are also disclosed.
WO2011022928A1 Quinolines compounds, their preparation methods, pharmaceutical compositions containing the same and use thereof Disclosed are disubstituted or trisubstituted quinoline compounds represented by the following general formula (I) or their pharmaceutically acceptable salts or solvates, which are used as c-Met inhibitors, their preparation methods, pharmaceutical compositions containing the same and uses of these compounds for preparing medicaments for preventing or treating diseases relating to cell abnormal proliferation and morphological variation associated with hepatocyte growth factor (HGFR) in organism, diseases relating to hyperkinesia and diseases relating to angiogenesis or metastasis, especially medicaments for treating or preventing tumor growth and metastasis.
EP2305260A1 Psychotropic agent and health food containing benzylisoquinoline derivative The present invention relates to a psychotropic agent for use in preventing and/or alleviating depression the agent comprising, as an effective ingredient, at least one compound selected from the group consisting of armepavin, O-methylarmepavine and pharmaceutically acceptable salts thereof.
WO2014030170A1 Acrylamide compounds as histamine h3 receptor ligands The present invention relates to novel acrylamide compounds of formula (I), and their pharmaceutically acceptable salts and process of their preparation. (The chemical formula should be inserted here.) The compounds of formula (I) are useful in the treatment of various disorders that related to Histamine H3 receptors.
WO2014039781A1 Treating hearing loss This invention relates to methods for treating hearing loss associated with loss of cochlear hair cells, e.g., caused by noise exposure, using certain gamma secretase inhibitors, in post-neonatal animals, e.g., adolescents and adults.
EP1355658B1 Anti HER3 antibody for diagnosis, prevention and treatment of hyperproliferative diseases The present invention relates to the use of a HER2 protein or a nucleic acid coding therefor as a target for the modulation of the mitogen-activated protein (MAP) kinase pathway. Further, the use of a PYK2 protein and a nucleic acid coding therefor as a target for the modulation of the MAP kinase pathway is described. By inhibiting HER3 kinase activity, the phosphorylation of PYK2 and thus the stimulation of the MAP kinase pathway is inhibited. The present invention is preferably suitable for applications, particularly diagnostic or medical applications, wherein an inhibition of the MAP kinase pathway is desired. Thus, the invention relates to novel methods for diagnosing, treating or preventing MAP kinase associated disorders such as tumors.
WO2008152994A1 Adsorbent for medical use It is intended to provide a spherical adsorbent carbon for medical use having high adsorption ability for a toxic substance and also high adsorption rate. The object was achieved by an adsorbent for medical use which is made of a granular phenol resin as a raw material and contains activated carbon in which the total amount of acidic groups is 0.16 meq/g or less, a weight loss rate when it is heated from 100˚C to 900˚C in a nitrogen atmosphere is 2% or less, the volume of pores with a diameter of 0.0075 to 15 μm is 0.1 to 1.0 mL/g, a BET specific surface area is 800 to 2000 m2/g, and an average particle size is 0.1 to 1.5 mm.
WO2014067379A1 Deuterated dimethyl amine parthenolide, preparation method and use thereof in drug preparation The present invention relates to a deuterated dimethyl amine parthenolide as represented by formula (I), preparation method and uses thereof in drug preparation, in particular to the uses thereof in the preparation of drugs for treating cancers and rheumatoid arthritis.
CN100584348C Anti-hepatitis medical combination Disclosed is a novel pharmaceutical composition for treating liver diseases and process for preparation, wherein the pharmaceutical composition mainly comprises glycyrrhizic acid or its pharmaceutically acceptable salts, tiopronin, kurarinone, one or more of silybin or its derivatives or silymarin, rhodiola rosea or rhodiola rosea, the composition can be prepared into any one of the pharmaceutically acceptable dosage forms, preferably injections and oral preparations.
US20110293549 Composition, method and kit for enhancing hair Compositions for application and methods of application of a composition to modify hair. In one embodiment, a composition includes a compound (molecule) represented by: wherein A and B are individually selected from a hydrogen, a hydroxyl group and a halogen, with the proviso that when one of A and B is a hydroxyl group, the other of A and B is a hydrogen and when one of A and B is a halogen, the other of A and B is a halogen or a hydrogen; wherein Z is, for example, an aryl moiety; and wherein X1 and X2 are, for example, individually selected from a hydrogen and an alkyl moiety, wherein R1 and R2 are individually selected from an oxo, a hydroxyl or an ester group; wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, or a salt.
CN101048399B 4-hetero aryl methyl substituted phthalazinone derivatives A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NRx or CRxRy; if X=NRx then n is 1 or 2 and if X=CRxRy then n is 1; Rx is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; Ry is selected from H, hydroxy, amino; or Rx and Ry may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are independently selected from the group consisting ofhydrogen and C1-4 alkyl, or when X is CRxRy, RC1, RC2, Rx and Ry, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R1 is selected from H and halo; and Het is selected from: (i) formula (i), where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N, where only one or two of Y1, Y2 and Y3 can be N; and (ii) formula (ii), where Q is O or S.
CN101926786A Sustained release preparation for cantharidin and cantharidin extract The invention discloses a sustained release preparation for cantharidin and cantharidin extract. The sustained release preparation is obtained by preparing solid dispersion from the cantharidin and cantharidin extract and then processing the solid dispersion, wherein the solid dispersion is prepared from the cantharidin or the cantharidin extract, PEG4000, PEG2000 or PVP, and is prepared by the following steps of: sieving and uniformly mixing the cantharidin solid dispersion, chitosan, MCC and starch; preparing a soft material from the mixture by using ethanol; sieving the soft material; drying the soft material at the temperature of 60 DEG C for 4 hours; and sieving the soft material with a 25-mesh sieve and granulating the soft material. The oral sustained release preparation of the invention can excellently control the cantharidin to keep the stable blood concentration in vivo, improve the bioavailability, reduce the toxic and side effect and relieve the irritation of mucous membrane.
WO2006131737A2 Method and composition for treating inflammatory disorders There is provided homogeneous pharmaceutical compositions for the treatment of inflammatory disorders comprising an antiinflammatory and/or antihistaminic active ingredient, a polar lipid liposome and a pharmaceutically-acceptable aqueous carrier.
US8269000 Substituted pyrimidine and triazine compounds Substituted pyrimidine and triazine compounds corresponding to formula I wherein R1, R2, R3, R4a, R4b, R5a, R5b, R7, R8, R9a, R9b, R10, R11, A, a, b, s, t, V, W1, W2 and W3 have defined meanings, pharmaceutical compositions comprising such compounds, a process for preparing such compounds, and the use of such compounds and compositions to treat or inhibit pain and/or other disorders or disease states.
WO2009098051A8 Aryl sulfonamides as effective analgesics The invention relates to compounds of general formula (I), in which A, B, R1, R2 and R3 are defined as cited in claim 1, to their enantiomers, diastereomers, their mixtures and their salts, in particular their physiologically compatible salts comprising organic or inorganic acids or bases that have valuable characteristics. The invention also relates to the production of said compounds, to drugs containing the pharmacologically effective compounds and to the production and use of said drugs.
CN102579484A Peritoneal dialysis solution for diseases caused by seawater immersion The invention discloses a peritoneal dialysis solution for diseases caused by seawater immersion. The peritoneal dialysis solution comprises 0.15 to 0.35 percent (w/v) of sodium chloride, 0.9 to 1.1 mmol/L of calcium chloride, 0.1 to 0.2 percent (w/v) of sodium lactate and proper amount of iso-osmia agent. The peritoneal dialysis solution is low in permeation pressure, can remove high sodium, high chlorine and high potassium brought by seawater and also can replenish water molecules for dehydrated tissues.
CA2714272A1 Therapeutic treatment for lung conditions Methods and compositions for treating lung conditions such as bronchopulmonary dysplasia or hypoxia-induced pulmonary hypertension in a subject, including administering to the subject an effective amount of a nitric oxide precursor such as citrulline.
US20090010885 Methods for Detecting and Treating Autoimmune Disorders The present disclosure relates to methods for inhibiting an autoimmune disease by administering to a subject a therapeutically effective amount of a composition that increases FOXP3 expression, thereby inhibiting the autoimmune disease. Further disclosed herein are methods for detecting in a subject an autoimmune disease or a predisposition to an autoimmune disease, and methods for assessing the efficacy of a therapy for an autoimmune disease.
CA2584489A1 Kaspp (lrrke) gene, its production and use for the detection and treatment of neurodegenerative disorders The present invention refers to a newly discovered gene named KASPP for Kinase Associated with Parkinsonism with Pleiomorphic Pathology or alternatively named LRRK2 for Leucine-Rich Repeat Kinase 2, its production, biochemical characterization and use for the detection and treatment of neurodegenerative disorders, such as Parkinson disease (PD) including, without limitation, sporadic PD, Alzheimer disease (AD), amyotrophic lateral sclerosis (ALS), and other synucleinopathies and/or tauopathy as well as several polymorphisms and mutations in the KASPP/LRRK2 gene segregated with PD.
CN103006702A Compound detoxifying agent for treating locoweed poisoning of livestock and preparation method of agent The invention relates to a compound detoxifying agent for treating locoweed poisoning of livestock and a preparation method of the agent. The compound detoxifying agent is prepared by dissolving an antidote into 1000 parts of sterilization water, and the antidote is prepared from the following components in part by weight: 0.25-0.5 part of yeast mannan, 0.8-1 part of L-rhamnose, 3-5 parts of magnesium sulfate and 8-10 parts of sodium orthophosphate. The compound detoxifying agent for treating locoweed poisoning of the livestock with the formula provided by the invention has definite components, is proven to have no toxic and side effect of teratogenesis, mutagenesis, carcinogenesis and the like by safety toxicology experiments, and is safe and reliable when being applied to production.
US20100093759 Bicyclic anilide heterocyclic cgrp receptor antagonists Compounds of formula I: I (wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
CN101804044B Abietate used for inhibiting helicobacter pylori The invention relates to an abietate used for inhibiting helicobacter pylori, the inhibition effect of which is better than that of a positive contrast--metronidazole, and the inhibition effect of a part of the abietate is the same as that of a positive contrast--amoxicillin, wherein the test result of the combination sample of 50% of abietic acid bismuth and 50% of amoxicillin and the combination sample of 50% of abietic acid sodium and 50% of amoxicillin is better than that of the positive contrast-amoxicillin, which indicates that the abietate and the amoxicillin have synergistic effect.
US20100331311 Galantamine as a neuroprotective drug for retinal ganglion cells The present invention relates to the use of galantamine for neuroprotection of retinal ganglion cells.
US20110034477 Crystalline Polymorph of Doxazosin Mesylate (Form IV) and Process for Preparation Thereof Crystalline Form IV of doxazosin mesylate, a process for its preparation and uses thereof.
US20110059102 Therapeutic Method Targeting Midkine Provided is a therapeutic method targeting midkine for treating mammalian kidney disorders, primary kidney disorders, hypertension that follows secondary kidney disorders such as diabetic nephropathy, and hypertension secondary to chronic kidney disease.
WO2014101067A1 Hypoglycemic compound and preparation method thereof, pharmaceutical composition comprising the hypoglycemic compound, and application thereof The present invention provides an antihyperglycemic compound and a preparation method thereof, a pharmaceutical composition comprising the antihyperglycemic compound, and an application thereof. The compound is a compound expressed in Formula (I) or a pharmaceutically acceptable salt, solvate, polycrystal, enantiomer, or racemic mixture thereof, wherein R1, R2, R3 and R4 are independently H, optionally substituted alkyl group, optionally substituted naphthenic base, optionally substituted alkyl sulphanyl, optionally substituted alkoxy group, optionally substituted aryl group, or optionally substituted aralkyl; or R1 and R2 together form optionally substituted naphthenic base; or R2 and R3 together form optionally substituted heterocyclic group; or R3 and R4 together form optionally substituted heterocyclic group. The compound is actively transported by a PepT1 transporter, then absorbed by gastrointestinal tract, and decomposed by enzyme in the intestinal tract and liver, to slowly generate Saxagliptin. Therefore, the plasma drug concentration of the Saxagliptin is increased or the staying time of the Saxagliptin in the blood is prolonged, and the stable plasma drug concentration improves the hypoglycemic effect and lowers side effects.
CN102351844B Pantoprazole sodium compound and pharmaceutical composition thereof The invention discloses a pantoprazole sodium compound, which is crystal. In X-ray powder diffraction pattern obtained through Cu-Kalpha ray measurement, the characteristic peaks of the pantoprazole sodium compound are shown in positions where 2theta is 12.5, 12.6, 13.2, 16.2 and 17.3. The pantoprazole sodium compound can be used together with multiple freeze-drying supporting agents, the prepared freeze-dried powder injection has the advantages of good redissolution, good transparency after redissolution, low impurity content and the like; and moreover, the use amount of the freeze-drying supporting agent is lower, thus saving the pharmaceutical cost and improving the stability of a drug preparation. The invention also discloses a pharmaceutical composition. The pharmaceutical composition comprises a pharmaceutical active ingredient and pharmaceutical auxiliary materials, wherein the pharmaceutical active ingredient is the pantoprazole sodium compound. The stability of the pharmaceutical composition is obviously superior to that of commercial products, and especially, the stability duration of the pharmaceutical composition after being matched with common infusion fluid is prolonged, thus facilitating the clinical application.
CN101386875A Synthesis of conjugate linoleate sugar esters derivates based on enzymatic method The invention relates to conjugated linoleic acid glucosyl ester derivatives, which mainly comprise conjugated linoleic acid glucose ester, conjugated linoleic acid maltose ester, conjugated linoleic acid lactose ester, conjugated linoleic acid fucose ester, conjugated linoleic acid sucrose ester,conjugated linoleic acid arabinose ester, conjugated linoleic acid fructose ester, conjugated linoleic acid galactose ester, conjugated linoleic acid seminose ester and so on. The products are prepared through the following steps: grease rich in a linoleic acid is taken as a raw material, and is subjected to alkali isomerization and molecular distillation purification to obtain a conjugated linoleic acid with higher purity, and then the conjugated linoleic acid is subjected to enzymatic catalysis reaction with saccharide compounds under normal temperature and normal pressure. The products are more stable than the conjugated linoleic acid, greatly improve shelf life, apparently improve the taste, enlarge application range, and can be widely applied to fields such as medicine, nutritional health products, food additives, functional feedstuff additives and so on.
WO2008087202A1 Triptolide derivatives for use in the treatment of acute myeloid leukemia The invention is directed to the use of an ester derivatives of triptolide, tripdiolide, 16-hydroxytriptolide, a pharmaceutically acceptable salt thereof, or a combination thereof, for the manufacture of a medicament comprising the triptolide prodrug for the treatment of acute myeloid leukemia.
US7776552 Drug screening; for inhibiting apoptosis in mammalian cells; zinc finger domains; consensus sequences; genetic engineering; for treating AIDS, alzheimer's disease, parkinson's disease, amyotrophic lateral sclerosis (ALS), retinitis pigmentosa, autoimmune diseases Disclosed is substantially pure DNA encoding mammalian IAP polypeptides; and methods of using such DNA to express the IAP polypeptides in cells and animals to inhibit apoptosis. Also disclosed are conserved regions characteristic of the IAP family and primer and probes for the identification and isolation of additional IAP genes. In addition, methods for treating diseases and disorders involving apoptosis are provided.
DE20221678U1 Preparation of an oxaliplatin active substance, useful in the treatment of cancer and comprising a very low content of oxalic acid Oxaliplatin active substance comprises oxalic acid (wt.%) (=0.8, preferably = 0.05, especially less than 0.02). An independent claim is included for the preparation of oxaliplatin active substance involving (a) Reacting potassium tetrachloroplatinate (K2PtCl4) with trans-l-1,2-cyclohexanediamine in an aqueous solution to obtain dichloro(trans-l-1,2-cyclohexanediamine)-platinum (II); (b) Adding silver nitrate (2 eq) to the product of step (A) to obtain diaquo(trans-l-1,2-cyclohexanediamine)-platinum (II); (c) Optionally adding potassium iodide or sodium iodide to the resulting solution, and adding active carbon under stirring; (d) Filtering and adding to the filtrate, alkali metal salt of oxalic acid, separating the oxaliplatin crystals formed by filtration and washing the crystals 2 - 5 times with water (pH 4.5 - 7); (e) Purifying oxaliplatin by recrystallisation to obtain crystals in a filter, where the crystals are washed 2 - 5 times with water (pH 4.5 - 7) to obtain the desired weight content of oxalic acid. - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : None given. -
EP1815850A1 Controlled release formulation of divalproic acid and its derivatives The present invention provides a controlled release dosage formulation comprising a) about 40% to about 80% of a valproic acid compound such as Divalproex Sodium and b) at least two, preferably hydrophilic, polymers each in an amount of less than about 20% of the dosage weight.
US20060127499 Vitamin-mineral compositions This invention provides compositions of vitamins and minerals used in the prevention and treatment of vitamin and mineral deficiency. These compositions provide a minimization of the intake dosage of vitamins and minerals while still meeting the nutritional daily requirements for these vitamins and minerals. At the same time, these compositions are easier to manufacture, have an improved prolonged shelf-life, and are easy and convenient to use. These compositions comprise 3 to 5 dose formulations that are ingested separately. Each dose formulation contains vitamins and minerals that are compatible with each other regarding systemic absorption and storage shelf-life.
CN101928259A 2-arylthiazole derivative and medicament composition thereof The invention designs and combines a 2-arylthiazole derivative with an xanthine oxidase inhibition activity, which has a chemical structure shown as (I), wherein Y represents O, S and NH; R1 represents H, C1-C4 alkane; R2 represents formacyl,-(CH2)nCO2H or -(CH2)nCOR5, wherein n=0-4, R5 is C1-C4 alkoxy or an amino acid; R3 represents formacyl, cyano, nitro, amino or hydroxamino; and R4 represents linear or branched C2-C8 alkenyl or conjugated or non-conjugated multi-alkenyl, linear or branched C2-C8 alkynyl or linear or branched and conjugated or non-conjugated C2-C8 alkenylalkynyl and pyridyl. The 2-arylthiazole derivative (I) is structurally characterized in that R4 in a substituent YR4 on an aromatic ring is unsaturated hydrocarbonyl. The 2-arylthiazole derivative has the activity of inhibiting xanthine oxidase, can be used for preparing a medicament for preventing and treating diseases, such as hyperuricemia, gout, and the like and has wide application in medicine.
WO2008001770A1 Antiallergic composition and agent, and food, beverage and animal feed each containing the composition or agent An anti-allergic composition or agent comprising β-1,4-mannobiose.
US20090076167 Deuterium-enriched tramiprosate The present application describes deuterium-enriched tramiprosate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2007046548A1 Pyrazolo[1,5-a]pyrimidine compounds as cannabinoid receptor antagonists The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), or a pharmaceutically acceptable salt thereof.
WO2011151251A1 New ccr2 antagonists The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (Ia) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
US20130040972 USE OF c-Src INHIBITORS IN COMBINATION WITH A PYRIMIDYLAMINOBENZAMIDE COMPOUND FOR THE TREATMENT OF LEUKEMIA The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) a pyrimidylaminobenzamide compound; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukemia, especially chronic myelogenous leukemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, in combination with a pyrimidylaminobenzamide compound, in particular 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide.
CN103083271A Analgesic tablet for pets The invention relates to a tolfenamic acid matrix tablet, which is composed of an active component tolfenamic acid, a high polymer material hydroxypropyl methyl cellulose (MethocelE4M), a filling agent and a lubricant. The tolfenamic acid sustained-release matrix tablet prepared in the invention has a good sustained release effect, a prolonged action time compared with ordinary tablets, and fewer adverse reactions. The preparation process involved in the invention has a simple process and a low cost, and can prepare products with stable quality, thus being suitable for industrialized production.
CN102670588A Application of ellagic acid to preparation of antiviral medicament The invention discloses an application of ellagic acid to preparation of an antiviral medicament. The virus refers to a simple herpes simplex virus and a human papilloma virus. The invention further discloses a medicinal composition taking ellagic acid as an active ingredient. A new way is opened up for the application of the ellagic acid.
CN1853666A Pharmaceutical, nutraceutical, dietetic and nutritional compositions based on vegetable fibres Pharmaceutical, nutraceutical, dietetic and nutritional compositions containing: a) glucomannan, b) Opuntia ficus indica , c) microcrystalline cellulose present a high gastrointestinal swelling index, which induces an immediate feeling of fullness, release of cholecystokinins and slowing of gastric voiding that prolongs the feeling of fullness. Associating the complex of three vegetable fibres with a mixture of freeze-dried mucilages increases its gastrointestinal swelling properties.
US20080075745 Topical pharmaceutical compositions containing ciclopirox or a pharmaceutically acceptable salt thereof Pharmaceutical topical oil in water type emulsion gels comprising ciclopirox or a pharmaceutically acceptable salt thereof are disclosed.
CN102558143A Derivant III of natural product Bostrycin and preparation method and purpose thereof The invention discloses a derivant III of a natural product Bostrycin and a preparation method and a purpose thereof. The derivant III of the natural product Bostrycin is provided with a structure of a formula (I), is linear alkyl and substitutional or non-substitutional phenyl with the formula that R12=H, OH; R13=H, Cl-C5 and is linear alkyl and substitutional or non-substitutional phenyl with the formula that R14=H, Cl-C5. The derivant of the natural product Bostrycin has good anti-tumor cell viability and can be further developed to be novel anti-tumor medicine as shown in the results of preliminary pharmacological researches (external anti-tumor cell tests).
CN103566032A Rheumatism ostalgia spray The invention relates to rheumatism ostalgia spray. Every 100 bottles of the rheumatism ostalgia spray comprises the following raw materials in volume: 10ml of lemon oil, 5ml of star anise oil, 3ml of safflower oil, 1ml of hot chilli oil, 5ml of camphor oil, 380ml of ethyl alcohol and 996ml of mixed propellant. The rheumatism ostalgia spray is easy to carry about and free from irritant to skin, and the rheumatism ostalgia treatment effective rate can be 96%.
EP1853599A1 Novel polymorph of mutilin Disclosed is a novel polymorphic form of the compound of formula (I) also known as mutilin 14-(exo-8-methyl-8-azabicyclo[3.2.1]oct-3-ylsulfanyl)-acetate, a process for the preparation of the polymorphic form, pharmaceutical compositions comprising the polymorphic form, and the use of the polymorphic form in medicine, particularly in antibacterial therapy.
WO2006056129A1 Compositions of huperzia serrata alkaloids comprising huperzine a and huperzine b and preparation thereof The present invention relates to the technical field of natural medicine. Specially, it relates to alkaloids extract of Huperzia serrata. The present invention provides compositions of Huperzia serrata alkaloids and preparation thereof. The present compositions of Huperzia serrata comprise Huperzine A and Huperzine B, in which the total content of Huperzine A and Huperzine B comprises 50% to 99% by weight of total alkaloids, the ratio of two being 1:0.5-5. The present compositions of Huperzia serrata alkaloids have good therapeutic effect and higher safety.
WO2005000303A1 Pyrazolo`3,4-b!pyridin-6-ones as gsk-3 inhibitors The invention provides compounds of formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein R1, R2, and R3 are as defined herein; pharmaceutical compositions thereof; and use thereof in the treatment of, inter alia, conditions, diseases, and symptoms such as diabetes, dementia, Alzheimer's Disease, stroke, schizophrenia, depression, hair loss, and cancer.
US20050176814 mono- or polydeuterated 4-(p-Methylsulfonylphenyl]-3-phenyl-2-(5H)-furanones; degenerative joint disorders, acute pain and primary dysmenorrhea The invention concerns deuterated substituted dihydrofuranones and pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated substituted dihydrofuranones for the treatment of symptoms for the irritating states of degenerative joint disorders, of acute pain and primary dysmenorrhea. In addition, the invention discloses pharmaceutical compositions, which contain deuterated substituted dihydrofuranones as well as their physiologically compatible salts, in addition to pharmaceutically compatible adjuvants and/or additives, for the treatment of symptoms for the irritating states of degenerative joint disorders, of acute pain and primary dysmenorrhea.
WO2006101535A1 Inhibition of proteasome function to potentiate the proapoptotic and antitumor activity of cytokines Disclosed herein are methods of using proteasome inhibitors to enhance an antitumor activity of a cytokine on a tumor cell that responds to treatment with the cytokine. Also provided herein are pharmaceutical compositions that include at least one cytokine and at least one proteasome inhibitor.
CN101239915A Beta-elemene monosubstituted amine derivatives, synthetic method and use thereof The invention discloses beta-elemene monosubstituted amine derivatives represented by formula I, and pharmaceutically acceptable salts thereof, wherein, R1 is H, R2 is n-butyl, tert-butyl, cyclohexyl, cyclopentyl, cyclooctyl, isopropyl, p-carboxylphenyl, p-carboxy phenoxyphenylmethyl or phenylmethyl; or both R1 and R2 are ethyl or -CH2COOH; or R1NR2 is imidazole. The invention also discloses a synthesis method of beta-elemene monosubstituted amine derivatives, comprising: dissolving beta-elemene chlorine substitutes and amine in solvent, and adding alkali catalysts to perform reaction. The invention further dicloses application of beta-elemene monosubstituted amine derivatives as reaction intermediates in synthesizing other beta-elemene derivatives, and in preparing anticancer drugs. Compared with beta-elemene, the beta-elemene monosubstituted amine derivatives of the invention have better water-solubility and higher anticancer activity.
US20090029967 Adenosine a2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless leg syndrome (RLS) or periodic leg movement in sleep (PLMS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS, dystonia, RLS or PLMS.
WO2010087107A1 Melanoma metastasis inhibitor Disclosed are: a practically useful melanoma metastasis inhibitor; a practically useful melanoma metastasis inhibition method; a use for preparing a practically useful melanoma metastasis inhibitor; and a practically useful screening method for a melanoma metastasis inhibitor. In the melanoma metastasis inhibitor, the melanoma metastasis inhibition method and the use for preparing a melanoma metastasis inhibitor, an SIRT1 inhibitory substance is used. The screening method for a melanoma metastasis inhibitor comprises the steps of: measuring the histone deacetylase activity of SIRT1 in the presence of a substance to be tested; comparing a value of the histone deacetylase activity obtained by the measurement with a value of the histone deacetylase activity of SIRT1 measured in the absence of the substance; and determining the substance as a melanoma metastasis inhibitor when the value of the histone deacetylase activity of SIRT1 measured in the presence of the substance is lower than that measured in the absence of the substance.
US8163303 Nutritional composition for the treatment of pressure ulcers The invention pertains to a method of treating or preventing pressure ulcers, comprising enterally administering to a subject in need thereof a composition comprising proteins, carbohydrates, fats, arginine or equivalents thereof, ascorbic acid equivalents and a-tocopherol equivalents, wherein arginine or equivalents thereof is administered in a daily amount of 3-15 g, ascorbic acid equivalents are administered in a daily amount of 180-840 mg and a-tocopherol equivalents are administered in a daily amount of 50-400 mg.
US20080124743 Diagnostics and therapeutics for diseases associated with neuromedin u1 receptor (u1) The invention provides a human NMU1 which is associated with the hematological diseases, cardiovascular diseases, disorders of the peripheral and central nervous system, inflammation diseases, cancer diseases, and disorders of the liver. The invention also provides assays for the identification of compounds useful in the treatment or prevention of hematological diseases, cardiovascular diseases, disorders of the peripheral and central nervous system, inflammation diseases, cancer diseases, and disorders of the liver. The invention also features compounds which bind to and/or activate or inhibit the activity of NMU1 as well as pharmaceutical compositions comprising such compounds.
CA2738755A1 Individual 5-fluorouracile dose optimization in folfiri treatment The present invention belongs to the field of improved personalized medicine. More precisely, the present invention relates to a method for progressively optimizing the 5 -FU dose administered by continuous infusion in patients treated by a FOLFIRI regimen or a similar regimen, based on the 5 -FU plasmatic concentration measured during the previous 5 -FU continu-ous infusion and on a herein described decision algorithm. The present invention also relates to a method for treating a cancer pa-tient in which the 5 -FU dose administered in continuous infusion in each FOLFIRI or similar treatment cycle is optimized using the decision algorithm according to the invention.
CN102090558A Composition containing probiotics, DHA (docosahexaenoic acid) and lactoferrin and applications thereof The invention relates to a composition containing probiotics, DHA (docosahexaenoic acid) and lactoferrin and applications thereof, the preservation registration number of lactobacillus plantarum LP-Onlly used in the composition is CGMCCNO. 1258, the preservation registration number of lactobacillus acidophilus LA-Onlly is CGMCCNO. 2106, and the preservation registration number of bifidobacterium longum BL88-Onlly is CGMCCNO. 2107. The composition contains the lactobacillus plantarum LP-Onlly, the lactobacillus acidophilus LA-Onlly and the bifidobacterium longum BL88-Onlly, as well as oligosaccharides, vitamins, the DHA, the lactoferrin and the like. The composition can be used as a food, a health care product or a medicament, is applicable to long-term consumption and is mainly used for regulating intestinal flora and enhancing the immunity.
CN102920834A Lvrong blood nourishing capsule and preparation method thereof The invention relates to a Lvrong blood nourishing capsule which comprises the following drug substances in part by weight: 108-132 parts of rhizoma atractylodis, 90-110 parts of angelica, 18-22 parts of pilose antler, 36-44 parts of prepared rhizome of rehmannia, 36-44 parts of tortoise shell, 72-88 parts of calcined copperas and 90-110 parts of medicated leaven. The invention further relates to a preparation method of the Lvrong blood nourishing capsule. The Lvrong blood nourishing capsule provided by the invention is a combination of seven herbs of rhizoma atractylodis, angelica, pilose antler, prepared rhizome of rehmannia, tortoise shell, calcined copperas and medicated leaven, has the effects of strengthening the spleen, tonifying the kidney, replenishing blood and nourishing blood, and is used for treating iron-deficiency anemia, which has symptoms of sallow complexion, dizziness, tinnitus, insomnia, amnesia, inappetence, fatigue, weakness, numbness of limbs and the like. The preparation method is simple and the cost of raw materials is low.
CA2352494C Compositions and methods for the treatment of alzheimer's disease, central nervous system injury, and inflammatory diseases The present invention relates to methods and compositions for treating Alzheimer's disease and other diseases and conditions with an inflammatory component (e.g., central nervous system injury). In particular, the present invention provides agents that regulate the production of proinflammatory and neurotoxic products involved in Alzheimer's disease and other diseases and conditions with an inflammatory component.
EP1335976B1 Modifier of organelle metalbolism The invention relates to a nucleic acid molecule encoding a polypeptide contributing to membrane stability and/or function of organelles, wherein said nucleic acid molecule (a) hybridizes under herein defined conditions to the complementary strand of a nucleic acid molecule encoding the amino acid sequence disclosed herein; (b) hybridizes under herein defined conditions to the complementary strad of a nucleic acid molecule as depicted herein; (c) it is degenerate with respect to the nucleic acid molecule of (a); (d) encodes a polypeptide which comprises at least one, preferably at least two, more preferably at least three, more preferably at least four, more preferably at least five and most preferably six amino acid sequences being part of the polypeptide contributing to membrane stability and/or function of organelles and comprising putative transmembrane region; (e) encodes a polypeptide which is at least 85%, preferably at least 90%, more preferably at least 95%, more preferabliy at least 98% and up to 99,6% identical to an amino acid sequence representing the above described polypeptide; (g) encodes a polypeptide which is at least 35%, preferably at least 50%, more preferably at least 60%, more preferably at least 70% more preferably at least 80%, more proferably at least 99%, most preferably at least 95% and most preferably at least 99% identical to the amino acid sequence as disclosed herein; (h) differs from the nucleic acid molecule of (a) to (g) by mutation and wherein said mutation causes an alteration, deletion, duplication or premature stop in the encoded polypeptide; or (i) has a sequence as disclosed herein.
CN101574375A Lactobacillus health-care capsule and preparation method thereof The invention relates to a lactobacillus health-care capsule with the health function and a manufacture method. The preparation method comprises the following steps: adopting two lactobacillus strainswhich are bred and selected from a human body as well as have the health-care efficacy and favorable production performance, enlarging and multiplying the lactobacillus strains through complex medium, making zymotic fluid into powder through a method of low-temperature cryodesiccation after fermentation is completed, and adding oligosaccharide powder according to a proportion to prepared the capsule. The lactobacillus health-care capsule is used through an oral method for people, can improve the gastrointestinal function, strengthen the immune function, promote absorption of nutrients, inhibit cancer cells, and delay aging. For adopting excellent strains, adding the oligosaccharide powder, and being manufactured into a capsule preparation, the invention can enhance the survival rate of thalli, and is preferable to embody the health-care efficacy. The invention is suitable for all people to use, exerts the health function, and is a safe and effective health-care food.
EP2639220A1 Indole derivatives and their use as antibiotics Compound of formula (I) or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof or a mixture of stereoisomers, which are useful as antibiotics. The invention also provides processes for the preparation of the compounds of formula (I) and intermediates, their compositions, their use as medicaments and methods for treating bacterial infections.
US20080293800 Cytotoxic Compounds and Conjugates The present disclosure provides cytoxic compounds useful as drugs or prodrugs and to drug-cleavable substrate conjugates where the drug and cleavable substrate are optionally linked through a self-immolative linker.
US20110275701 Anti-thrombin aptamer formulations and methods for use The invention relates to the formulation, dosing, administration and use of an aptamer antagonist therapeutic that binds to thrombin.
US7422733 Antiinflammatory agents; anticancer agents; antidiabetic agents Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl Lex, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.
US7612059 Pyrrolidine bicyclic compounds and its derivatives, compositions and methods of use N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
US20080096946 Tetramethylation of 3,5-di(cyanomethyl)toluene, oxidation of the 1-methyl group to form an aldehyde, conversion to a Boc-protected hydrazone, reduction to a Boc-protected hydrazine, salt formation, conversion to anastrozole; industrial scale, high yield and purity; anticarcinogenic agent; breast cancer A process for the preparation of anastrozole.
CN1969983A Quality control method of cough-stopping (Ke Ke) capsule The invention discloses a quality control method for cough-relieving capsules, which comprises conducting part or total items of description, authentication, inspection and content determination, the authentication including microscope inspection, thin layer chromatogram identification of Chinese ephedra and licorice root, and content determination being conducted to morphia in poppy capsule. Compared with the prior arts, the quality control method provided by the present invention can achieve high accuracy, better repeatability, high recovery ratio, and accurate measurement result.
US20110105490 2,3-dihydro-1h-isoindol-1-imine derivatives useful as thrombin par-1 receptor antagonist The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists.
WO2012135641A2 Aurora kinase inhibitors and methods of making and using thereof Described herein are inhibitors of Aurora kinase and their use in the treatment of cancer. Methods of screening for selective inhibitors of Aurora kinases are also disclosed.
US20080171706 Anti-Adhesive Compounds to Prevent and Treat Bacterial Infections The present invention provides compounds and compositions capable of inhibiting the attachment of Gram-negative bacteria on a host epithelium. Accordingly, said compounds and compositions can for example be used for the manufacture of a medicament to treat urinary, lung and gastrointestinal infections caused by said Gram-negative bacteria
CN1634048A Berberine hydrochloride granule for masking flavor and its preparation The invention discloses a berberine hydrochloride granule for masking flavor and its preparation which comprises flavor concealing dressing material and berberine hydrochloride bundled therein, wherein the total amount of berberine hydrochloride is 45-65% of the total amount of flavor concealing berberine hydrochloride, the preparation comprises, (1) film forming material, selected from one or more of Eudragit E100, Eudragit EPO, Eudragit L100, and methyl hydroxypropylcellulose, which amounts to 70-80% of the total weight of the flavor concealing dressing material, (2) plasticizing agent, which is selected from one or more of PEG6000, dibutyl sebacate, triethyl citrate, whose amount is 5-15% of the total weight of the flavor concealing dressing material, (3) antistatic agent selected from one or more of magnesium stearate, talcum powder, micro powder silica gel, whose amount is 5-15% of the total weight of the flavor concealing dressing material.
WO2006071995A9 Serine amino acid derived prodrugs of propofol, compositions, uses and crystalline forms thereof The present invention provides a prodrug of propofol and crystalline forms thereof, methods of making the propofol prodrug and crystalline forms thereof, pharmaceutical compositions of the propofol prodrug and crystalline forms thereof, methods of using the propofol prodrug and crystalline forms thereof and pharmaceutical compositions thereof to treat diseases or disorders such as headache pain, post chemotherapy or post operative surgery nausea and vomiting, neurodegenerative disorders, and mood disorders.
US20100074897 Methods and Compositions related to HIF-1 alpha Disclosed are compositions and methods related to HIF-1α.
CN101899008B N-substituted pyrimidine sulfonyl-substituted benzamide type small molecular inhibitor for Bcl-2 protein and application thereof The invention relates to an N-substituted pyrimidine sulfonyl-substituted benzamide type small molecular inhibitor for an antiapoptotic member of Bcl-2 protein family and an application thereof. The N-substituted pyrimidine sulfonyl-substituted benzamide type compounds related in the invention are represented in the formula 1 and have the action of inhibiting the antiapoptotic member of Bcl-2 protein family (such as Bcl-2, Bcl-xL, Mcl-1 and the like), and the detailed definition of each group is shown in the specifications. The compounds (and stereoisomers thereof if existing), medicinal salts thereof, hydrates thereof, solvates thereof and medicinal compositions thereof can be used for treating diseases or symptoms related to the high expression of the antiapoptotic member of Bcl-2 protein family, or can be used for treating tumors or can be used as an synergist or used together with other antitumor medicines for treating tumors. The invention also relates to compounds represented inthe formula 1 and a preparation method of the medicinal salts.
CN101428025B New use of anti-impaludism medicament hydroxyl chloroquine The invention relates to the novel usage of an antimalarial medicine, in particular to the novel usage of hydroxychloroquine having sensitivity enhancing effect on various chemical anti-multiple myeloma medicaments. The novel usage is characterized in the application of hydroxychloroquine in treatment of multiple myeloma through chemotherapeutic medicaments. The hydroxychloroquine can obviously enhance the killing activity of chemotherapeutic medicines such as doxorubicine, epidoxorubicin, cis-platinum and mitoxantrone to multiple myeloma cells, and the killing activity thereof is realized byinhibiting the myeloma cell autophagy signals by hydroxychloroquine. Hydroxychloroquine can induce the quantity of the autophagy lysosomes of the multiple myeloma cells to be increased and the expression of the autophagy-associated albumen LC3-II to be increased.
EP1189522B1 Use of nanoscale sterols and sterol esters The invention relates to the use of nanoscale sterols and/or sterol esters with particle diameters of between 10 and 300 nm as food additives and as active agents for producing hypocholesterolaemic products. The invention is characterized by the particular fineness of the particles compared to sterols and sterol esters of the prior art. This results in quicker resorption through the serum with oral administration.
US20120039913 Selective Histamine H4 Receptor Antagonists for the Treatment of Vestibular Disorders The invention relates to Histamine H4 receptor antagonists or inhibitors of Histamine H4 receptor gene expression for the treatment and/or the prevention of vestibular disorders.
US20110038829 Methods and materials for treating diarrhea This document relates to methods and materials for administering bile acid sequestrants to treat conditions associated with diarrhea. For example, formulations designed for the delivery of a bile acid sequestrant (e.g., colesevelam) to treat diarrhea are provided.
EP1517673A1 Nasal composition comprising a mucopolysaccharide and propylene glycol The invention relates to pharmaceutical compositions adapted to nasal administration. The nasal formulations of the invention are characterized inter alia by having excellent moisturizing properties and not requiring a preservative.
CN103405400A Levosulpiride injection and preparation method thereof The invention discloses a levosulpiride injection and a preparation method thereof. The preparation method is characterized by comprising the following steps: selecting a biodegradable encysting material; smashing levosulpiride powder to nanopowder; and preparing a slow release nanocapsule injection under an ultrasonic condition. The purpose of quick effect, stable effect and long effect is realized, the half-life period is prolonged, the compliance is improved, the product stability is increased, and the promising result is obtained.
US20080280979 Methods and Compositions of Derivatives of Probucol for the Treatment of Diabetes This present invention provides methods and pharmaceutical compositions for the treatment or prophylaxis of diabetes and related disorders, comprising the administration of an effective amount of a monoester of probucol, particularly the monosuccinic acid ester, or a pharmaceutically acceptable salt or derivative thereof.
CN1739560A Dietotherapeutic product for preventing and treating urate calculi, gout and acalcerosis and its prepn process The dietotherapeutic product for preventing and treating urate calculi, gout and acalcerosis consists of salt of organic acid, salt of inorganic acid, vitamin and trace elements. The dietotherapeutic product operates on that the product creates conditions for dissolving urate in water soluble alkali salt and removing and for dissolving calcium salt in acid solution for being absorbed and utilized, and the vitamin and the trace elements reinforce the activity of enzyme, protect the functions of cell and organ, recover nucleotide and make purine to synthesize essential nucleic acid to reduce purine and urate and avoid urate calculi and gout. The dietotherapeutic product has obvious curative effect, no toxic side effect, simple preparation process, and low cost.
CN101273047A Thieno[2,3-B]pyridine-5-carbonitriles as protein kinase inhibitors Disclosed are compounds of Formula I: Formula (I); wherein R<1>, R<2>, R<3>, R<4> , and X, are defined hereinbefore in the specification, which can be useful in the treatment of autoimmune and inflammatory diseases, and processes for producing said compounds.
CA2362932C Pharmaceutical composition containing proton pump inhibitors The present invention is concerned with an oral pharmaceutical formulation containing a proton pump inhibitor (PPI) which is suitable for the treatment of gastric acid related diseases in man and animals. More specifically, the composition is a paste, and is particularly suitable for delivery of a proton pump inhibitor to horses.
WO2010048358A3 Ethoxyphenylmethyl inhibitors of sglt2 The present invention relates to new ethoxyphenylmethyl modulators of SGLT2, pharmaceutical compositions thereof, and methods of use thereof. (Formula I)
EP2123260A1 Liposome formulation and process for preparation thereof A liposomal pharmaceutical formulation comprising multivalent ionic drug, a process for the preparation thereof, and the use thereof in the treatment of diseases, wherein the particle size of the liposome is about 30-80 nm, and the phospholipid bilayer contains a phospholipid with Tm> body temperature thereby the phase transition of the liposome is above body temperature.
US6998231 Coding or classification of prion sample; obtain sample, monitor physical properties of sample, compare to control The present invention relates to a method for typing a sample of a prion or spongiform encephalopathy disease, a kit suitable for use in such a typing method, a method for identifying infection in an animal and/or tissue of bovine spongiform encephalopathy (BSE), a method for assessing and/or predicting the susceptibility of an animal to BSE, a kit for use in such an assessment and/or prediction method, a method for the treatment of a prion disease, and compounds suitable for such a method.
WO2009098208A1 Novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1]octane and their use as monoamine neurotransmitter re-uptake inhibitors This invention relates to novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1 ]octane useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
US7335651 Controlling concentration of cholesterol, leptin, and serotonine in blood; dietetics; adjust fat oxidation Methods for promoting healthy body weight and improving a variety of related physiological factors, including serum serotonin levels, serum leptin levels, fat oxidation, cholesterol levels, and body mass index, in persons or other mammals, include administering to those persons or other mammals effective amounts of hydroxycitric acid or a combination of hydroxycitric acid, chromium and gymnemic acid, which work synergistically to further to promote healthy body weight and improve these physiological factors.
CN101380321A Compounds, formulations, and methods for ameliorating telangiectasias In methods, compounds, and topical formulations for treatment of rosacea, compounds represented by the formulas below are incorporated: wherein each of R1, R2, and R3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R4 and R5 is independently hydrogen, alkyl, or alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A1, A3, and A4 is independently hydrogen or alkyl; and A2 is independently hydrogen or hydroxy; and wherein each of B1, B2, and B3 is independently hydrogen, hydroxy, or alkoxy; and each of B4 and B5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat rosacea and its symptoms.
CN101328186A Thienopyrimidine and thienopyridine derivatives useful as anticancer agents The invention relates to compounds of formulas (1) and (2) and to pharmaceutically acceptable salts and hydrates thereof, wherein X<1>, R<1>, R<2> and R<11> are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas (1) and (2) and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formulas (1) and (2).
US7122572 For use in Hydrogen Bonding Liquid Chromatography, environmental remediation by removal of undesired ions or neutral molecules, removal of phosphate for kidney dialysis, drug delivery, separation The present invention provides calixpyrrole, calixpyridinopyrrole, and calixpyridine macrocycles, having 4, 5, 6, 7, or 8 heterocyclic rings, as well as syntheses, derivatives, conjugates, multimers, and solid supports thereof. Such macrocycles have proved to be effective and selective ion- and neutral molecule-binding agents forming supramolecular ensembles, and ion- and neutral molecule-separation agents. The macrocycles are fully meso-non-hydrogen-substituted porphyrinogens, a few molecules of which were previously known but not recognized as possessing anion- or molecule-binding properties. The binding mode is noncovalent, primarily that of hydrogen-bonding, thereby providing a new mode for liquid chromatography, that of Hydrogen Bonding Liquid Chromatography. Further useful applications of the macrocycles provided herein include environmental remediation by removal of undesired ions or neutral molecules, and removal of phosphate for kidney dialysis.
US7220740 1,4-diazabicyclo[3.2.2]nonabenzoxazole, -benzothiazole and benzimidazole derivatives, preparation and therapeutic use thereof Compound corresponding to the general formula (I) in which X represents an oxygen or sulphur atom or an NH group and R1, R2, R3 and R4 each represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, trifluoroalkoxy, cyano, hydroxyl, (C1–C6)alkyl, (C1–C6)alkoxy or phenyl group. Application in therapeutics.
CN102602949A Preparation method of mineral-fiber-free montmorillonite The invention relates to a preparation method of mineral-fiber-free montmorillonite, which is characterized by adopting the following steps of: selecting crude ores of bentonite and adequately drying, soaking in water, blending and washing, separating by a water cyclone and dehydrating to obtain the mineral-fiber-free montmorillonite. According to the preparation method, the safety of the montmorillonite can be improved.
WO2010089874A1 Ppar-γ-expression-enhancing agent, adiponectin-production-enhancing agent, ucp-activating agent, and pharmaceutical preparation, food or beverage comprising any one of the agents Disclosed are: a PPAR-γ-expression-enhancing agent which comprises procyanidin B2 as an active ingredient and has an activity of enhancing the expression of PPAR-γ; an adiponectin-production-promoting agent which comprises procyanidin B2 as an active ingredient and has an activity of promoting the production of adiponectin; an UCP-activating agent which comprises procyanidin B2 as an active ingredient and has an activity of enhancing the expression of UCP; an anti-diabetes agent, an anti-obesity agent, an agent for reducing the accumulation of a visceral fat or an agent for inhibiting the accumulation of a visceral fat, which comprises any one of the PPAR-γ-expression-enhancing agent, the adiponectin-production-promoting agent and the UCP-activating agent; and a food or beverage comprising any one of the PPAR-γ-expression-enhancing agent, the adiponectin-production-promoting agent and the UCP-activating agent. It becomes possible to provide a pharmaceutical preparation, a food or a beverage which does not cause any adverse side effect, is harmless for a human body, and is expected to have an effect of enhancing the expression of PPAR-γ, an effect of promoting the production of adiponectin, an effect of enhancing the expression of UCP, an effect of ameliorating obesity, diabetes or the like which is induced by the effect of enhancing the expression of PPAR-γ, the effect of promoting the production of adiponectin or the effect of enhancing the expression of UCP, or the like.
CN102134267A Novel dehydropachymic acid The invention discloses a novel compound. The compound is dehydropachymic acid and has good anti-dementia activity.
CA2379995C 11.beta.-aryl-17,17-spirothiolane-substituted steroids The invention is directed to a novel class of 11.beta.-aryl-17,17-spirothiolane-substituted steroid compounds exhibiting binding to the progestin receptor.
CN102188674A Health-care liquid for promoting blood circulation, removing blood stasis and freeing bi The invention relates to health-care liquid for promoting blood circulation, removing blood stasis and freeing bi, and relates to ingredients and a preparation method of health-care liquid. The technical problem to be solved is to provide the ingredients and the preparation method of the health-care liquid for promoting the blood circulation, removing the blood stasis and freeing the bi. The ingredients of the health-care liquid comprise the following raw materials: nutgrass galingale rhizome, costustoot, fennel, clove, fortune eupatorium herb, suberect spatholobus stem, yanhusuo, borneol, notoginseng root, prepared common monkshood daughter root, incised notopterygium rhizome, pubescent angelica root, dried ginger, camphor, Mongolian dandelion herb and 60 degree distilled spirit. The preparation method comprises the following steps of: a, preparing materials; b, grinding the ingredients into powder, and sieving with a 60-mesh sieve; c, immersing the ingredients in the 60 degree distilled spirit in a weight ratio for 3 hours, and removing impurities. The method is applied to the preparation of the health-care liquid. Underwear is immersed in the health-care liquid, and is aired and dressed to achieve the health-care effects of promoting the blood circulation, removing the blood stasis, dispelling wind and clearing damp, freeing the bi and easing pain and activating the blood circulation.
CN101185640A Lomoxicam sustained release tablet and preparation method thereof The invention provides a lornoxicam sustained release tablet and the preparation method thereof. The sustained release tablet includes 2.0-60.00 parts of lornoxicam by weight and 10.00-95.00 parts of sustained release block material by weight; wherein, the sustained release block material includes hydroxypropyl methyl cellulose or compound of hydroxypropyl methyl cellulose and other celluloses. The preparation method is that raw material prescription doses of lornoxicam, sustained release block material and filler are evenly mixed, then added with adhesive to be prepared into soft material; pelletization, drying and finishing granule are carried out according to the conventional technique of the tablet preparation, and the dry grain after finishing granule is added with lubricant, evenly mixed and pressed to make the preparation. Compared with conventional oral lornoxicam preparation, the lornoxicam sustained release tablet can maintain a longer effect after oral administration of the drug.
CN101249266B Nano liver target direction amphipathic nature block copolymers drug administration system and preparation The invention relates to a drug delivery system of nanometer liver targeting amphiphilic block copolymer and a preparation method thereof. The nanometer liver targeting drug delivery system is obtained by adopting liver targeting amphiphilic block copolymer which can be biologically degraded and which has good biocompatibility as the carrier material and embedding drugs for treating liver diseasesby a solvent dialysis method or a solvent evaporation method; the weight ratio of the carrier material to the drug is 1:0.1 to 1.2. The drug delivery system has the advantages of simple operation, mild condition and cheap raw material; the prepared drug delivery system has good biocompatibility and both effects of active targeting and passive targeting, and can realize high targeting and sustained release drug delivery to the liver by means of injection, thus solving the defects of bad targeting and low bioavailability of present anticancer drugs and improving the life quality of patients, with broad application prospects.
CN102202666A Therapeutic uses of compounds having affinity to the serotonin transporter, serotonin receptors and noradrenalin transporter Therapeutic uses of 4-[2-(4-methylphenylsulfanyl)phenyl]piperidine and therapeutically acceptable salts thereof are provided.
CN103357023A Method for increasing solubility of 10-hydroxycamptothecin, product prepared by the method and applications of the product The invention relates to methods of preparing medicaments by a medicine inclusion technology, belongs to the field of pharmaceutical preparation technology, and particularly relates to a method for increasing solubility of 10-hydroxycamptothecin, a product prepared by the method and applications of the product. The invention discloses a solid inclusion compound 10-hydroxycamptothecin (HCPT)/cucurbit[7]uril (Q[7]) formed by including 10-hydroxycamptothecin and cucurbit[7]uril. By dissolving the solid inclusion compound in water, the solubility of the 10-hydroxycamptothecin is increased by 1642-2565 times. Preparation methods of the solid inclusion compound comprise A. a co-evaporation method, B. a grinding method and C. a freeze-drying method. The preparation methods for the inclusion compound are simple and the solubility of the 10-hydroxycamptothecin in water can be greatly increased, thus reducing medicine dosage, reducing medicine taking duration and frequency, shortening courses of treatment and reducing medicine toxic and side effects for patients who take the 10-hydroxycamptothecin for treatment.
US7034032 1,2,3-triazolo(4,5-d)pyrimidine compounds used to treat cardiovascular disorders The invention provides novel 1,2,3-triazolo[4,5-d]pyrimidine compounds, such as those represented by formula (I): their use as medicaments, particularly in platelet aggregation disorders, compositions containing them and processes for their preparation.
US6867213 Vitronectin receptor inhibitors; bone diseases, osteoporosis; esterification of acid form with isopropanol (2S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use The present invention relates to (2S)-2-(adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester of the formula I and its physiologically tolerable salts, their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them. The compound of the formula I and its physiologically tolerable salts are valuable pharmacologically active compounds which can be used, for example, in the treatment or prophylaxis of diseases which can be influenced by inhibiting the vitronectin receptor, for example of bone diseases such as osteoporosis.
US6977244 Inhibition of Bcl-2 protein expression by liposomal antisense oligodeoxynucleotides The present invention provides novel compositions and methods for use in the treatment of Bcl-2-associated diseases like cancer, specifically, in the treatment of follicular lymphoma (FL). The compositions contain antisense oligonucleotides that hybridize to Bcl-2 nucleic acids, the gene products of which are known to interact with the tumorigenic protein Bcl-2. Used alone, or in conjunction with other antisense oligonucleotides, these compositions inhibit the proliferation of FL cancer cells.
WO2011144248A1 Composition for removing atheromatous plaque The invention relates to a mixture of two active principles for removing atheromatous plaque, i.e. procaine of formula (I) and a pharmaceutically acceptable alkoxysilane or aryloxysilane and more particularly monomethyltrisilanol salicylate of formula (II), where the hydrogen bonds linking the OH functions of the silanols to the phenol functions of salicylic acid are sufficiently strong for preventing, even at high temperatures, the polycondensation and hence the non-solubilization of the monomethyltrisilanol salicylate (the active principle of a drug sold under the trademark « CONJONCTYL »). The proportions of the two active principles of the composition, which can be delivered intramuscularly, range from 30 to 60 ml of monomethylytisilanol salicylate for 3 to 10 ml of procaine. The frequency of the injections is defined by treatments of 20 to 40 sessions.
CN101204418A Application of Cajanus cajan L. extracts on preparating hyperlipemia medicine The invention discloses a new medical use of an extract of pigeon pea leaves, in particular to provide the application for preparing medicine used for treating hyperlipemia and fatty liver as well as the application for preparing the health products used for lowering hyperlipemia and fatty liver.
US7169819 A pharmaceutical formulation for parenteral delivery, comprising a retinide such as fenretinide in combination with a solvent (an alcohol) and a alkoxylate castor oil, capable of dispersing or dissolving the retinide; anticancer agent A pharmaceutical composition for parenteral delivery, comprising a retinide such as fenretinide in combination with a solvent capable of dispersing or solubilizing the retinide. The solvent comprises an alcohol, such as ethanol, in combination with an alkoxylated castor oil, such as CREMOPHOR® EL, or comprising a retinide, such as fenretinide, in an emulsion composed of a lipoid dispersed in an aqueous phase, a stabilizing amount of a non-ionic surfactant, optionally a solvent, and optionally an isotonic agent. In addition, a method of use in the treatment of hyperproliferative disorders, such as cancers is described.
EP2556057A1 7,11-methanocycloocta [b]quinoline derivative as highly functionalizable acetylcholinesterase inhibitors The present invention concerns new highly functionalizable Huprine derivatives of formula I: a method for preparing such compounds and their use for treating neurological diseases in which the level of acetylcholine is affected such as Alzheimer's disease.
CN1526023B Use of primer and probe of aldose reductase gene in preparing composition for determination of risk factors for cataract This invention relates to methods for determining the risk of developing cataract in mammals, and, more specifically, in mammals, including humans, with non-insulin dependent diabetes. The methods are performed by determining the presence or absence of genetic markers in genomic DNA. The presence of a Z-2 allele, a microsatellite marker of the aldose reductase, is indicative of an increased risk for developing cataract. The presence of Z-4, a microsatellite allele of the aldose reductase gene, indicates a decreased risk for developing cataract. The methods comprise nucleic acid probes that hybridize to a nucleic acid encoding the microsatellite region of the mammalian aldose reductase gene. The probes may also be immobilized on a solid support to form a microarray. In addition, this invention is directed to methods for treating a mammal with a genetic predisposition for developing cataract; following a screening method that detects a Z-2 microsatellite marker of an aldose reductase gene the mammal is treated with an inhibitor of aldose reductase.
WO2010115230A1 Immunogenic composition and uses thereof The present invention provides an immunogenic composition comprising an antigen and a dendritic cell targeting component. A charged group is covalently attached to a dendritic cell ligand and is electrostatically associated with the dendritic cell targeting component.
WO2005011648A3 Use of cyclic bioisosteres of purine system derivatives for the treatment diseases caused by disorders of nitrergic and dopaminergic systems The invention relates to compounds of general structural formula (I), wherein R= formula (II), Li, Na, K; R1= -H, -NH2, -Br, -Cl, -OH, -COOH; B=-N=,-CH=, Z=-CH=,-N=; A=-N at B= -N=, Z=-CH-; A=-CH = at B= -N=, Z;=-CH-; A=-CH = at B= -N=, Z=-N=; A=-CH = at B=-CH=, Z=-CH=; A=-CH = at B=-CH=, Z=-N= and to the pharmacologically acceptable salts thereof used in the form of an active ingredient exhibiting an activity with respect to nitrergic and/or dopaminergic systems for pharmacological compounds in the form of a neuroprotector, for improving a cognitive function, normalising a psychophysiological state and for treating a largerange of neuropsychic and cardiovascular diseases, and diseases caused by a substance abuse and by a hyperactive immune system of mammals including a human being.
WO2012004875A1 Novel substance separated from orchidaceous plant, and extract, antioxidant, antibacterial agent, anticancer agent and antiinflammatory agent containing same [Problem] To provide an antioxidant which has an effective antioxidant effect without showing any side effects. [Solution] A novel substance represented by formula (1).
US20090317475 Combination antitumor therapies Improved methods of treating cancers that are characterized by unwanted angiogenesis employ combinations of therapies designed to inhibit the VEGF mediated angiogenesis pathway with therapies designed to inhibit the bFGF-mediated angiogenesis pathway.
US20050245545 administering a xanthine derivative such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methylxanthine The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof. More preferably the adenosine A2A receptor antagonist is a xanthine derivative or a pharmaceutically acceptable salt thereof.
WO2009026680A1 Supramacrqmolecular polymer complexes providing controlled nitric oxide release for healing wounds A bio-adhesive supramacromolecular complex of the general formula (1): wherein R1 is an alkane unsubstituted or substituted with alkoxy groups; R2 is a lower alkane; R3 and R4 are long chain, optionally substituted, alkanes; W is a hydrogen-bond accepting functional group-containing entity; Y is a carboxylic acid ester or amide; Z is a linking group; T1, T2, T3 and T4 are terminal groups; and m1, m2, n1 and n2 are integers selected from at least 25; and wherein P has a molecular weight of about 1 x 103 to 1 x 107 and Q has a molecular weight of about 1 x 103 to 1 x 107. The complex provides controlled nitric oxide release over a longer period of time than prior art compounds in the locally delivery systems. Novel compositions, methods of preparation, apparatus including layer-by-layer assemblies coating, electrospinning and ultrasonic atomization, skin coverings containing and medical use of the complexes are described.
US20090069297 protein kinase inhibnitors such as N-(4-((7-(methyloxy)-1,5-naphthyridin-4-yl)oxy)phenyl)-4-phenyl-1-phthalazinamine, for influencing the process of cell cycle and cell proliferation to treat cancer; anticarcinogenic agents The present invention relates to chemical compounds having a general formula I wherein A1-8, D′, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
CN1806806A Leponex dispersible tablet and preparation method thereof The invention discloses a clozapine dispersion tablet, which is prepared from 50.0-65.0 wt% of clozapine, 1.0-3.0.0wt% of sodium carboxymethylstarch, 25.0-40.0.0wt% of crystalline cellulose, 0.1-0.5.0wt% of Aspartame, 0.2-1.0.0wt% of magnesium stearate, 0.1-0.5wt% of sodium dodecyl sulfate, 2.0-4ú«0% of polyvinylpyrrolidone and 1.0-3.0% of miropowdered silica gel through disintegrating and passing through 100 mesh sieve, mixing homogenously, adjusting sheet weight, tabletting so as to obtain the dispersible tablets.
US7629340 N-(6-membered aromatic ring)-amido anti-viral compounds Disclosed are compounds having Formula (I) and the compositions and methods relating to these compounds, for treating or preventing a viral infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R2, m, R, V, W, T, Z, R1, Y, and p are disclosed herein.
WO2009066325A1 Controlled release pharmaceutical compositions of pregabalin A controlled release pharmaceutical composition which comprises therapeutically effective amount of pregabalin or salts thereof as active ingredient, a hydrophobic release controlling agent(s) and optionally other pharmaceutically acceptable excipients thereof.
WO2005077936A1 Pyridine benzimidazole sulfoxides with high purity A method for preparing a pyridine benzimidazole sulfoxide compound having the formula (I) with the step of oxidizing a pyridine benzimidazole thioether compound with an oxidation agent, during that oxidation step a pyridine benzimidazole sulfone compound is formed as an undesired by-product. It is proposed to stop the oxidation step prior the amount of undesired pyridine benzimidazole sulfone product exceeds 1,0 %-by weight based on the entire amounts of compounds.
US8653064 Crystalline forms of sodium 4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-D][2]benzazepin-2-yl]amino}-2-methoxybenzoate The present invention is directed to a compound of formula (I): or a crystalline form thereof, or a solvate thereof; to a solid pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and at least one pharmaceutically acceptable carrier or diluent, and to the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a disease, disorder, or condition mediated by Aurora kinase, and methods related thereto.
CN101977594A Method for the identification of patients in need of therapy having minor cognitive disorders and the treatment of such patients A method for the identification of patients in need of therapy and for the preventive treatment of such patients having minor cognitive disorders, wherein an increased risk can be determined for said patients to develop clinically manifested Alzheimer's disease during a preceding risk stratification as a result of an increase in circulation-relevant peptide biomarkers measurable in the circulation of said patients, using drugs that comprise one or more active ingredients of cardiovascular agents, which are selected from the group consisting of ACE inhibitors, angiotensin II receptor antagonists, betablockers and blood pressure-lowering diuretics and the combinations thereof, or using drugs comprising one or more ANP receptor antagonists or one or more adenosine receptor antagonists.
US7148242 N-formyl hydroxylamine compounds, compositions and methods of use N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes or imidazacyclo4-7alkanes have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections.
CN101006975B An oral medicine preparation containing salvianolic acid A and extract of panax natoginseng, and its preparation method and application The invention discloses a salvianolic acid A and notoginseng extract preparation for oral administration, its preparing process and use thereof, characterized in that the preparation comprises salvianolic acid A and Notoginsen triterpenes by a weight ratio of 1:1-10, preferably 1:3, the weight ratio of salvianolic acid A and notoginseng panaxadiol saponin is 1:1-5, the weight ratio of salvianolicacid A and notoginseng panaxadiol saponin Rb1 is 1:0.5-5. The preparation has good pharmaceutical actions.
WO2006049078A1 Drug for external use for treating skin disease It is intended to provide a drug for external use which can make an affected part less conspicuous or cover the affected part by actively removing scuff, etc. formed by the hyperproliferation of skin cells while showing lessened side effects due to heat damage or excessive drug absorption at the affected part. This drug for external use for treating a skin disease is characterized by containing an emulsion type adhesive component, water and a drug for treating a skin disease.
WO2007135163A1 Use of poly(hexamethylene biguanide)hydrochloride as an antiviral agent The invention relates to the use of poly(hexamethylene biguanide)hydrochloride as an antiviral agent, in particular in the production or treatment of a polymer or textile article. The invention also relates to an article which has been treated with antiviral agent and to a method for the production of such an article. The article can be, for example, a textile or a plastic, in particular, a polyurethane.
CN103126976A Terbinafine hydrochloride cream and preparation method thereof The invention relates to a terbinafine hydrochloride cream. According to the invention, terbinafine hydrochloride with an effective amount is adopted as a main raw material, and the cream is prepared with the main raw material and pharmaceutically acceptable auxiliary materials of sodium dodecyl sulfate, propylene glycol, glycerol monostearate, octadecanol, white vaseline, light liquid paraffin, ethyl paraben, and water. The cream provided by the invention has the advantages of moisturizing cream body, good spreadability, convenient medication, low irritation to skins, good treatment effect, and stable quality.
CN103006552A Formulation process of adenosine cyclophosphate for injection The invention discloses a formulation process of adenosine cyclophosphate for injection and provides a formulation process which has the advantages of low cost, high yield and more stable end product quality. The formulation process comprises the following steps: (1) taking water for injection, 50 percent of the expected formulation quantity, cooling the water below 40 DEG C, adding mannitol, stirring to ensure complete resolution, adding medical charcoal, 0.3 percent (W/V) of the expected formulation quantity, uniformly stirring, standing 30 minutes, removing carbon, filtering and cooling below 20 DEG C; (2) adding anhydrous adenosine cyclophosphate into the filtrate obtained in the step (1), stirring while dripping 10 percent of sodium hydroxide solution to enable the anhydrous adenosine cyclophosphate to be completely resolved, and adjusting the pH value of the solution to 5.8-6.2; and (3) supplementing water for injection, below 20 DEG C, to 1,000ml, uniformly stirring, re-testing that the pH value ranges from 5.8 to 6.2, sequentially filtering the solution through 0.45 Mum and 0.22 Mum microporous filtering films, and after inspecting that the semi-finished product is qualified, sending for filling. The formulation process enhances the product market competitiveness, facilitates product marketing and is worthy of popularization.
CN101309915A Compounds and compositions as lxr modulators The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
US20080058367 Process for the purification of palonosetron or its salt The present application relates to a process for purification of palonosetron or its salt substantially free of its R-isomer and structure related impurities.
US6987121 Compositions and methods for hepatoprotection and treatment of cholestasis Methods for the treatment of cholestatic liver disease and reduction and prevention of hepatic injury resulting from cholestasis via administration of a FXR ligand are provided.
US7074814 Antiinflammatory agents; cardiovascular disorders; anticancer agents; antiarthritic agents ; psoriasis The present invention provides indoles of Formula I: wherein R1 and R2 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
CN103070843A Oral preparation containing andrographolide and preparation method thereof The invention relates to an oral preparation containing andrographolide and a preparation method thereof, belonging to the field of medicines. The oral preparation containing andrographolide is in dosage forms of enteric-coated granules, enteric-coated tablets, enteric-coated capsules and enteric-coated dispersible tablets which are prepared by mixing andrographolide and pharmaceutically acceptable auxiliary materials. The prepared oral preparation can reduce incidence of adverse reactions and side effects thereof and improve the medication safety while ensuring the therapeutic effect, and uses the andrographolide more widely.
CN101584698A 6H-thiochromeno[4, 3-d][1, 2, 4]triazolo[1, 5-a] pyrimidine serial synthetic medicine with anticancer activity The invention discloses a sulfur-nitrogen contained four-ring heterocyclic compound, particularly a 6H-thiochromeno[4, 3-d][1,2,4]triazolo[1, 5-a] pyrimidine compound with anticancer activities. Aiming at the current research and development situations of few anticancer medicines with large toxicity in the prior art, the 6H-thiochromeno[4, 3-d][1, 2, 4]triazolo[1, 5-a] pyrimidine compound anticancer experiment is made, and an RPMI Medium 1640 is used as a cell culture medium and a detecting method which is an MTT method is adopted in the experiment. An experimental result indicates that the compound has high anticancer activities in vitro and can be used as the anticancer medicine.
CN102366423B External compound drug for treating burn and scald The invention discloses an external compound drug for treating burn and scald. The external compound drug is prepared from the following medicinal raw materials: 60 of calcined calamine, 3 of mercurous chloride, 10 of borneol, 0.2 of streptomycin sulfate and 0.2 of penicillin. The external compound drug is prepared by uniformly mixing the medicinal raw materials, co-pulverizing, screening by using a 300-mesh sieve, and bottling the drug powder for later use. The drug disclosed by the invention has the advantages of low cost, easily available drug sources, rapid curing effect on burn and scald, obvious effect and no scar left after curing. By using the drug to treat burn and scald, the effect is obvious, the burnt and scalded skin syndromes are rapidly eliminated, the use is convenient, notoxic, side or irritation action exists, the effective rate is 100%, and the curative rate is 97%.
CN101168050B Immunity regulating medicinal composition Provided is a composition of immunological regulation medicines. Each medicine dose unit contains interleukin 25u to 1500u, interferon 15u to 1000u, thymosin 0.5ug to 25ug, transfer factor 0.00002u to 0.0015u and hydrocortisone 30ug-150ug. Taking poultry eggs as adhesive agents, the medicines are added in the poultry eggs, are further well mixed, are dried, and are comminuted into powder, and the powder was encapsulated to finish the production. The composition of the medicines is capable of inducing and stimulating the immune response, thereby achieving the purposes of healing, disease prevention and health care. The active constituent dosage is minute in quantity, thereby being without any adverse poison deputy reaction. By observing the curative effect of abdominal smooth muscle spasm,allergic purpura, diabetes and megrim, the effect is satisfied.
WO2006016657A1 Drug for treating or preventing hcv infection By discussing the HCV replicon inhibitory activities of compounds originating in microorganisms such as one belonging to the genus Aureobasidium, myriocin, fumonisin B1 and a ceramide transportation inhibitor HPA-12, it is observed that these compounds have effects of inhibiting the replication of HCV replicon RNA or inhibiting the expression of the HCV protein. By performing a knockdown experiment on serine palmitoyl transferase with the use of siRNA, it is found out that the HCV replicon activity and the expression of the HCV protein are significantly inhibited in cells wherein the expression of LCB1 is regulated, suggesting that sphingo lipid biosynthesis might participate in HCV infection. Based on these facts, it is clarified that HCV infection can be treated or prevented by inhibiting an enzyme activity occurring in the process of sphingo lipid biosynthesis by the addition of a compound or the knockdown of a gene.
WO2006042850A1 Cyanothiophenes, the production thereof and their use as medicaments The invention relates to cyanothiophenes of general formula (I), in which the R's are defined in the claims, and relates to their tautomers, stereoisomers, mixtures and salts that have valuable pharmacological properties, in particular, a glucagon receptor-antagonistic action.
WO2014044869A2 Medical preparation comprising a carrier and polyhexanide or octenidine The invention relates to pharmaceutical compositions and in particular medical preparations that contain a carrier and an antiseptic, wherein the antiseptic is selected from the group comprising polyhexanide, octenidine, and mixtures thereof. The invention further relates to various products that have a medical preparation according to the invention and to specific uses of the medical preparation.
CN101385720A Sitafloxacin hydrate capsules and preparation method thereof The invention relates to a sitafloxacin capsule and a production method thereof, each tablet contains 25-200mg of sitafloxacin and pharmaceutical excipients, the pharmaceutical excipients mainly comprise 2 parts of starch, 0.5 part of microcrystalline cellulose and lubricant; the preparation method is as follows: the sitafloxacin, the starch and the microcrystalline cellulose are evenly mixed and then granulated, the lubricant is added after the granulation, and the capsule filling is carried out. The product has the advantages of stable quality, convenient carry and drug delivery as well as fast dissolution of active ingredients.
CN101287733A Novel isoindole derivatives, compositions containing same, preparation thereof and pharmaceutical uses thereof in particular as inhibitors of chaperone protein Hsp90 activities The present invention concerns novel products of formula (I), wherein: A1, A2, A3 and A4 represent CRa or N; n represents 1 or 2; R1 represents O, S or NRb; R2 represents H, halogen, CF3, nitro, cyano, methyl, ethyl, hydroxy, mercapto, amino, methoxy, thiomethoxy, methylamino, dimethylamino, acetylamino, carboxy and carboxamido; Ra represents in particular H, halogen, CF3, hydroxy, mercapto, nitro, amino, NH-OH, NH-CO-H, NH-CO-OH, NH-CO-NH2, carboxy, cyano, carboxamido, Y-(CH2)p-alkyl, Y (CH2)p-cycloalkyl, Y-(CH2)p-heterocycloalkyl, Y-(CH2)p-aryl or Y-(CH2)p-heteroaryl, with Y = O, S, NH, O-C(O), C(O)-NH, NH-C(O), NH-S(O) or NH-S(O)2, and p = 1, 2, or 3; Rb represents H, (CH2)m-cycloalkyl, (CH2)m-heterocycloalkyl, (CH2)m-aryl or (CH2)m-heteroaryl, with m = 0, 1, 2; said products being in all isomeric forms and the salts thereof, as medicines.
US20080167369 Semisynthesis Process for the Preparation of 10-Deacytyl-N-Debenzoyl-Paclitaxel The invention relates to a process for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel, a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. The invention also discloses a process for the preparation of Docetaxel starting from said compound of formula (I).
WO2014076338A1 Use of a photosensitive agent capable of producing reactive oxygen species in the production of a drug for the photodynamic therapy of a disease related to stem cells, in vitro use, and pharmaceutical composition The invention relates to the use of a photosensitive agent, or the precursor thereof, capable of producing reactive oxygen species (ROS) in the production of a drug that can be used for the photodynamic therapy (PDT)-based treatment of a disease related to a patient's stem cells, preferably epidermal stem cells.
CN101942034B Non-insulin-dependent diabetes mellitus-resisting liriope spicata fructosan and preparation method and application thereof The invention provides liriope spicata fructosan consisting of nineteen beta-D-fructose and one alpha-D-glucose. The liriope spicata fructosan comprises a main chain consisting of fructose residues bonded at positions 1 and 2 and six repeating units, wherein each unit comprises one disubstituted fructose residue bonded at positions 1 and 2, one trisubstituted fructose residue bonded at positions 1, 2 and 6 and one monosubstituted fructose residue bonded at position 2; and hydroxyl at position 2 at one terminal of the main chain of a polysaccharide is bonded with hydroxyl at position 1 of the alpha-D-glucose to form a glycoside, and hydroxyl at position 1 at the other terminal of the main chain of the polysaccharide is bonded with hydroxyl at position 2 of one beta-D-fructose to form a glycoside. The liriope spicata fructosan has the advantages of capacity of obviously reducing the blood glucose of mice suffering from non-insulin-dependent diabetes mellitus and the insulin resistance, reducing the total cholesterol and triglyceride in blood, increasing the ratio of high-density lipoprotein to low-density lipoprotein better and more effectively preventing and treating arteriosclerosis and thrombosis, wherein the strength of the insulin resistance and that of rosiglitazone do not have any statistical difference.
CA2813570A1 Porphyrin treatment of neurodegenerative diseases Compositions and methods of treating a neurodegenerative disorder are disclosed herein.
CN101066949A Prepn process of organic salt of coculine for diminishing inflammation and relieving pain The present invention discloses preparation process of organic salt of coculine for diminishing inflammation and relieving pain. The preparation process includes dissolving organic acid of non-steroid anti-inflammatory analgesic and coculine in the same molar amount in proper amount of alcohol, reflux reaction for about 1 hr, and eliminating solvent to obtain the organic salt of coculine for diminishing inflammation and relieving pain. The non-steroid anti-inflammatory analgesic is selected from aspirin, salicylic acid, Brufen, etc, and the organic salt of coculine for diminishing inflammation and relieving pain has the function of lowering the untoward reactions of non-steroid anti-inflammatory analgesic and bioavailability higher than coculine.
CN103127103A Application of sophoridine in anti-tumor drug preparation The invention belongs to the field of chemical engineering and medicine, and relates to an application of sophoridine in anti-tumor drug preparation. The present invention provides an application of sophoridine in anti-tumor drug preparation, wherein tumor cells comprise leukemia cells and pancreatic cancer cells. The sophoridine belongs to natural products, and has characteristics of low toxic-side effect, high bioavailability, stable property, and clinical use value. With application of the small molecule compound as a new anti-tumor drug or an auxiliary component thereof to be developed, advantages of significant tumor inhibition effect and green environmental protection are provided, and a new way is provided for treatment and cure of tumors.
CN103333064A Loxoprofen sodium compound and pharmaceutical composition thereof The invention belongs to the technical field of medicine, and particularly relates to a loxoprofen sodium compound. The structural formula of the loxoprofen sodium compound is as follows: the loxoprofen sodium compound is measured through Cu-K alpha rays, and an X-ray powder diffraction spectrogram is obtained and shown as a figure 1. The loxoprofen sodium compound has low possibility of moisture absorption and has very excellent liquidity, so that the accuracy of subpackage is improved, and the loxoprofen sodium compound and other ingredients can be easily and uniformly mixed. The invention further provides a preparation method of the loxoprofen sodium compound and a pharmaceutical composition containing the loxoprofen sodium compound. The pharmaceutical composition can be prepared into a granule, a tablet or a capsule, preferably the capsule. Finally, the invention further provides a preparation method of the pharmaceutical composition.
EP1027056B1 Alpha-ketoamide multicatalytic protease inhibitors This invention relates to α-ketoamide inhibitors of multicatalytic protease (MCP), to compositions including such inhibitors, and to methods for the use of MCP inhibitors. The MCP inhibitors of the present invention are useful, for example, to retard loss of muscle mass incident to various physiological states.
WO2014017462A1 Pharmaceutical composition for inhibiting abnormal spine formation It is now revealed that the amount of syntenin protein is increased in tuberous sclerosis. It is now also revealed that the binding between syndecan-2 protein, which is a protein known as a factor capable of inducing the formation of spine, and CASK protein is inhibited with the increase in the amount of syntenin protein to cause abnormal spine formation. It is found that abnormal spine formation in tuberous sclerosis can be inhibited, abnormal behavior can be improved and the occurrence of epileptic seizure can be prevented by administering siRNA specific to syntenin gene. Thus, provided are: a pharmaceutical composition and a vaccine composition both for inhibiting abnormal spine formation; and a method for screening for a compound having an activity of inhibiting abnormal spine formation.
US20110021562 Treatment of friedreich's ataxia using histone deacetylase inhibitors The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.
EP1808432B1 Amorphous form of cinnamide compound An amorphous object of (3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4methyl-1H-imidazol-1-yl)benzylidene]piperidine-2-one, which is represented by the formula (1) and has Aβ-production inhibitory activity. The amorphous object has such satisfactory properties that it has excellent solubility, is stable, does not readily become a crystalline form, and has low hygroscopicity. It is hence suitable for use in pharmaceutical preparations.
CN103083249A Method for preparing berberine chitosan drug-carrying microsphere by salting-out process The invention discloses a method for preparing a berberine chitosan drug-carrying microsphere by a salting-out process. With berberine as a model drug, the method disclosed in the invention adopts the salting-out process, takes unmodified chitosan as a packing material, and employs sodium tripolyphosphate as a cross-linking agent to prepare the berberine chitosan drug-carrying nanoparticle successfully. The invention has the advantages that: no modification on chitosan is needed in advance, the berberine is packed through the salting-out process, the operation is simple, the repeatability is strong, and no toxic or side effect exist. Due to the special properties of chitosan, modification and grafting of other molecules on its surface are easy, thus making targeted transport and metabolic study of packed drugs possible.
US7393933 Hepatitis B monoclonal antibodies A monoclonal antibody that is capable of binding specifically to wild type HBsAg and to at least two mutant forms of HBsAg may be used in an improved immunoassay for the detection of both escape mutants and wild type HBsAg and may be used for passive immunisation against HBV.
EP2785683A1 Inkt cell modulators and methods of using the same Disclosed herein are α-galactosylceramide (α-GalCer) analogs and compositions thereof, methods of activating invariant Natural Killer T (iNKT) cells using said analogs, methods of treating diseases by activating iNKT cells using said analogs, and combination therapy of said analogs.
US20110104287 Fenoldopam formulations and pro-drug derivatives Formulations of fenoldopam are disclosed for repeated administration or continued slow release administration, over prolonged periods of time or targeted slow and regulated delivery. The formulations include those formulations that increase the bioavailability of fenoldopam after oral intake, particularly lipid based nano dispersions and pronanodispersions and surfactant rich formulations. This may be accomplished by entrapment in nanoparticles or liposomal formulations or conjugation to a polymer or small molecule via a soft bond.
US20090143437 Ep4 receptor antagonists Compounds of formula (X): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(═O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted alkyl; (iv) tetrazol-5-yl.
WO2014102619A3 Compositions of aluminum fluoride and methods of use thereof for the treatment and prevention of actinic keratosis and sun-induced damages The present invention is directed to methods and compositions for the treatment or prevention of actinic keratosis and/or for countering the effects of skin aging and/or damage to blood vessels and fine wrinkling. The present invention provides for a composition comprising aluminum fluoride or chemical compounds which releases aluminum fluoride to be used to treat or reduce the negative effects of actinic keratosis or sun-induced skin aging and associated conditions, for example, damaged blood vessels and fine wrinkling.
CN101518511A Method for preparing ophthalmic preparation containing tacrolimus The invention discloses a method for preparing a preparation containing tacrolimus, which comprises the following steps of: using absolute ethyl alcohol to dissolve the tacrolimus first wherein the mass ratio range of the tacrolimus and the alcohol is 0.01-0.5g: 0.01-2ml; adding a solubilizing agent and/or a stabilizing agent which is dissolved in water for injection; then adding a thickening agent and/or a bacteriostat, and supplementing the water for injection to the needed volume; or then adding a well-dissolved eye ointment matrix to obtain the preparation containing the tacrolimus. The preparation containing the tacrolimus prepared by the method has the advantages of good solubility, small irritation, stable characteristics, no toxic side effect, and the like.
WO2009138582A3 Use of a composition containing 7-dehydrocholesterol or a natural extract of a vegetable or animal microorganism The invention relates to the cosmetic use or use as a food-additive of a composition that contains 7-dehydrocholesterol, a 7-dehydrocholesterol derivative, or a natural extract of a vegetable or animal microorganism containing the same, in order to protect cells against the consequences of an oxidative stress such as an exposure to ultraviolet, particularly solar, radiation, and in order to prevent the occurrence of senescent cells losing the reproductive capabilities thereof and having adverse effects on the surrounding tissues.
US8383636 Acyclic amine inhibitors of 5-methytioadenosine phosphorylase and nucleosidase The present invention relates to compounds of the general formula (I) which are inhibitors of 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.
US20110229584 Compound for the control of herpes simplex virus using glycyrrhizic acid, lipoic acid, allantoin, and slippery elm A Theraputic composition of glycyrrhizic acid, slippery elm, zinc oxide, allantoin, lysine monohydrochloride, L-Carnitine, Lipoic acid, Salicylic Acid, Citric Acid, vitamin E Acetate, wheat germ oil, and Shea butter for the treatment of HSV-1, HSV-2, canker sores, shingles, and other epidermal and oral ailments.
US20130225653 Microrna-based short hairpin rna for gene knockdown of nr1 subunit of n-methyl-d-aspartate receptor and its application on pharmaceutics The present invention relates to a microRNA-based short hairpin RNA for gene silencing the genetic expression of NR1 subunit of N-methyl-D-aspartate receptor comprises a single strand RNA fragment comprising a first fragment, a second fragment and a connecting fragment, wherein the first fragment and the second fragment are complementary to each other, and are spaced and connected by the connecting fragment, with the connecting fragment being randomly arranged nucleotides, with the first fragment having a Drosha recognized cleavage site, a silencing site and a Dicer recognized cleavage site, with the Drosha recognized cleavage site and the Dicer recognized cleavage site being spaced and connected by the silencing site, with the silencing site encoding homologous nucleotides corresponding to NR1 subunit of subcutaneous N-methyl-D-aspartate receptor.
CN101274897A Crystalline polymorphs of desvenlafaxine succinate and their preparations The present invention relates to two new polymorph Form V and Form F of desvenlafaxine succinate, to processes of their preparations, pharmaceutical composition comprising such materials and their use in therapy. Form V of desvenlafaxine succinate is prepared from recrystallizing desvenlafaxine succinate in a mixture of tetrahydrofuran (THF) and methanol ethanol, butanol, isopropyl alcohol, propanol, or the mixture of the combination by crystallized solvent. Form F of desvenlafaxine succinate is obtained from recrystallization of desvenlafaxine succinate in a mixture of cyclohexane and one or more of polar or nonpolar organic solvent or the mixture of any combination.
CN101485642B Method for preparing compound controlled release capsule for treating benign prostatic hyperplasia and the compound controlled release capsule The invention discloses a method for preparing a compound controlled-release capsule for treating benign hyperplasia of prostate and the compound controlled-release capsule for treating the benign hyperplasia of prostate, and belongs to the technical field of medicines. The method comprises that: common micro pills containing the finasteride medicine and slow release micro pills containing the doxazosin pills are prepared respectively, and the two kinds of micro pills are mixed and encapsulated to prepare the controlled-release capsule, wherein the mass ratio of the finasteride medicine to the doxazosin medicine in the capsule is 1:0.625-2.5. In the method, ethylcellulose and hydroxypropyl emthylcellulose are used as auxiliary materials of the slow release preparation, and by combining the preparation process by which the auxiliary materials is mutually cooperated with compound medicines, the finasteride-doxazosin compound controlled-release capsule is prepared. Active ingredients in the two medicines in the preparation not only can be mutually cooperated to achieve better curative effects, but also can stably release the medicines, avoid the difference between blood concentrationat wave crest and wave hollow, and reduce toxic and side effects of the medicines on human body; moreover, the controlled-release capsule can also shorten the medicine taking time of patients and improve compliance of taking medicines. The finasteride-doxazosin controlled-release capsule can be used as the medicine to treat hypertension and benign hyperplasia of prostate.
US20080305095 Nutritional Drink A first composition of drink ingredients specifically designed to lower cholesterol that addresses multiple mechanisms including hepatic synthesis and release, intestinal absorption of cholesterol, while, at the same time, including ingredients that mitigate the side effects of the constituents and increase their efficacy by affecting emotional factors that influence compliance such as a sense of well-being and euphoria on the one hand, or an increased overall metabolism and desire for the product stemming from its coloration on the other hand.
US20120129805 Barley and uses thereof The invention provides barley gain comprising a reduced level or activity of starch synthase IIa protein and a starch content of at least 41% (w/w) and methods of producing, identifying and using same. The grain may comprise an amylase content of at least 50%, a β-glucan content of 5-9% (w/w) or greater than 9% (w/w), and/or a fructan content of 3-11% (w/w). The fructan may comprise a degree of polymerization from about 3 to about 12. For example, the plant and grain comprises a sex6-292 allele and/or an amo1 mutation. A food or beverage product, and methods of producing a food or beverage product, comprising obtaining or producing the subject grain and processing the grain to produce the product. Also contemplated are methods of improving one or more indicators of health in a mammal comprising administering a composition comprising the subject barley grain or a product comprising same.
US7087615 Antiinflammatory agents; antiarthritic agents The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; each R2 unit is independently selected from the group consisting of: a) hydrogen; b) —(CH2)jO(CH2)nR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —(CH2)jCON(R10)2; g) —(CH2)jOCON(R10)2; h) two R2 units can be taken together to form a carbonyl unit; i) and mixtures thereof; R8, R9a, R9b, and R10 are each independently hydrogen, C1–C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; j is an index from 0 to 5, n is an index from 0 to 5; Z is O, S, NR11, or NOR11; R11 is hydrogen or C1–C4 alkyl.
US7078402 Sulfur compounds such as S-methyl 4-dimethylamino-4-methyl-2-pentynethioate, used for prophylaxis of cancers, skin disorders or vision defects The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.
CN103120685A Application of Aphanamixoid A in medicine for increasing erythrocytes The invention discloses a new application of a compound Aphanamixoid A in the field of medicine preparation, and particularly relates to an application of the Aphanamixoid A in preparation of a medicine for increasing erythrocytes. The application of the Aphanamixoid A in preparation of the medicine for treating erythrocyte lack is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on erythrocyte lack is inconceivably high; and the Aphanamixoid A has outstanding substantiality characteristic without possibility of any inspiration given by other compounds and obviously achieves the outstanding progress by being used for preventing and treating the erythrocyte lack.
US7038049 Anticancer agents; antitumor agents; apoptosis of breast tumor cells; drug resistance leukemia The present disclosure includes compounds, for example a compound according to formula I or a pharmaceutically acceptable salt thereof. The compounds of the present disclosure are useful in methods of treating cancerous conditions.
CN1559416A Dripping pills of acetyl-gastrodin, and prepn. method therefor A dripping pill of acegastrodine is prepared from acegastrodine and medicinal carrier chosen from polyethanediol, polysorbate, polyoxyvinyl stearate, gelatin, steaic acidand sodium stearate through proportionally mixing chosen carriers, heating while stirring, adding acegastrodine, stirring while heating to 100 deg.C, dripping in condensing medium, condensing, and drying in air.
CN102397230A Bathing cream for curing scapulohumeral periarthritis The invention discloses a bathing cream for curing scapulohumeral periarthritis, which relates to the technical field of bathe goods; the preparation process comprises the steps of: taking the formula medicinal materials of 3% of saussurea involucrata, 4% of camphora wood leaf, 5% of lycopodium clavatum, 5% of garden balsam stem, 3% of geranium wilfordii, 4% of cassia twig, 3% of turmeric, 4% of angelica, 3% of lucid ganoderma, 4% of rhizome atractylodis, 3% of ligusticum wallichii, 4% of divaricate saposhnikovia root, 5% of achyranthes bidentata, 2% of dried orange pee, 2% of red yeast rice, 1% of liquorice to be mixed with millet wine and be soaked for two times, the soaking liquid medicines of the two times are combined and mixed together uniformly; the medicinal material residues are continuously added with water to decoct for three times, the decoction liquids of the three times are combined and mixed together and uniformly, and are carried out alcohol precipitation, the supernatant fluid is uniformly mixed with the soaking liquids of the first time, the liquid medicine is heated to concentrate into cream, then 10% of deep sea mineral salt, 10% of deep sea algae, 5% of safflower, 3% of pine oil and an appropriate amount of millet wine are added, uniformly mixed, packed, vacuumized and sealed. The bathing cream for curing the scapulohumeral periarthritis can effectively cure the scapulohumeral periarthritis, accelerate blood circulation, improve physical fitness, dispel mild wind, dredge collaterals, clear heat, detoxicate, nourish blood, invigorate blood circulation, clear damp, eliminate blood stasis, is not toxic, has no side effect, and can build bodies.
CN1962681A A plurality of antineoplastic sapogenin and its injection preparation method The invention discloses a saponin compound to prevent tumour preparing method of its agent, which comprises the following steps: adopting panaxoside, American ginseng saponin, Notoginsen triterpenes and gynostemma pentaphylla saponin as raw material; dissolving in the high-boiling point organic solvent; aerating oxygen to do oxide alkaline degradation; adsorbing product through column chromatography to obtain protopanaxadiol, protopanaxatriol and Octoid.
WO2006113376A1 2 -aminocarbonyl substituted piperazine or diaza-cyclic compounds as apoptosis protein inhibitor (iap) modulators The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases.
US20100247645 Pharmaceutical combination of aliskiren and valsartan The present invention relates to a pharmaceutical oral fixed dose combination comprising a) a therapeutically effective amount of Aliskiren, or a pharmaceutically acceptable salt thereof, b) a therapeutically effective amount of Valsartan, or a pharmaceutically acceptable salt thereof, wherein the pharmaceutical oral fixed dose combination shows an in vitro dissolution of component (a) of 60% or less after 10 minutes and 95% or less after 20 minutes, and a dissolution profile of component (b) of 25% or more after 30 minutes, and 45% or more after 60 minutes at pH 4.5, said pharmaceutical oral fixed dose combination being bioequivalent to a free dose combination of Aliskiren and Valsartan.
US20130065928 Biomarkers for pi3k-driven cancer Disclosed is the discovery that the mTORC2 complex plays a role in the regulation of PKN3 phosphorylation at the turn motif threonine; and the use of the phosphorylation status of the turn motif threonine of PKN3 as a biomarker. In some embodiments, the phosphorylation status of the turn motif threonine of PKN3 is determined using an antibody that specifically binds to the turn motif threonine of a PKN3 protein, such as an anti-phosphoT860 antibody. In some embodiments, the invention relates to methods for screening compounds that have cancer therapeutic potential, methods for diagnosing cancer, methods for determining the prognosis of a patient suffering from cancer, methods for stratifying patients in a clinical trial, methods for treating a patient suffering from cancer, and methods for determining the effectiveness of a particular treatment regimen.
CN102531893A Shikonin octyl methoxycinnamate derivant as well as synthesis method and application thereof The invention belongs to the technical field of the chemical pharmacy, in particular to medicine design which takes shikonin as a primer and a relevant research for antitumor activity. A series of substituted cinnamic acid is introduced into a shikonin skeleton molecule by a synthesis means to obtain a corresponding ester derivant. The in-vitro antitumor activity research shows that the shikonin octyl methoxycinnamate derivant has strong inhibitory activity on tumor cell strains.
WO2012174243A1 D -serine for the treatment of visual system disorders The present invention relates to therapeutic methods using pharmaceutical compositions comprising one or a combination of co-agonists at the N-methyl-D- aspartate receptor for the treatment of visual system disorders.
CN102516350A Glycyrrhetinic acid modifier with antitumor activity and preparation method thereof The invention relates to a glycyrrhetinic acid modifier with antitumor activity and a preparation method thereof, which relate to structural modification technology of glycyrrhetinic acid. The method comprises the following step that: after carrying out esterification on 30-bit carboxyl and alkyl chloride of the glycyrrhetinic acid, modifying an A loop to realize structural modification of the glycyrrhetinic acid so as to obtain a series of glycyrrhetinic acid derivatives (I 1-5, I I1-5, III 1-5, IV 1-5 and V1-5). Through a test, the glycyrrhetinic acid modifier has a certain inhibiting effect for human body cervical carcinoma HeLa cells, hepatocelular carcinoma HepG2 cells and gastric cancer BGC-823 cells. The structure of the glycyrrhetinic acid derivatives is shown in the figure below.
CN103181896A Liposome preparation comprising berbamine medicine, and preparation method thereof The invention belongs to the field of medicine preparation, and specifically relates to a liposome preparation comprising a berbamine medicine, and a preparation method thereof. The liposome comprises the berbamine medicine, phospholipid, cholesterol, a hydrophilic lipid derivative, and a gradient establishment substance. A mass ratio of the medicine to phospholipid is 1:5-1:100, a mass ratio of cholesterol to phospholipid is 1:2-1:4, and a mass ratio of the hydrophilic lipid derivative to phospholipid is 1:2-1:6. The preparation method provided by the invention is feasible. With the method, the quality is controllable, such that the method is suitable for industrialized productions. The obtained berbamine medicine liposome has small particle size, uniform particle distribution, high encapsulation rate, and good stability. When the berbamine medicine is prepared into liposome, medicine blood circulation time can be effectively prolonged, tumor tissue targeting efficiency can be improved, and medicine in-vivo antitumor effect is enhanced. Or, a synergetic antitumor effect can be developed with the liposome and other chemotherapy medicines, toxicity can be reduced, and body immunity can be improved.
US20130040958 Imatinib mesylate preparation procedure Methods for making Imatinib mesylate of formula (I): having low levels of organic solvent are provided. Also provided are alpha and beta forms of Imatinib mesylate and methods for treating conditions such as chronic myelogenous leukaemia by administering same.
US20120172401 Benzimidazole derivative and use as angiotensin ii antagonist The present invention provides (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-cyclopropyl-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate represented by the formula: which has superior properties as a pharmaceutical agent, a salt thereof, a crystal thereof, a pharmaceutical agent containing the compound, and the like.
CN102861060A Application of Houttuynoid B in leukemia treatment medicine The invention relates to application of Houttuynoid B in preparing leukemia treatment medicine, which belongs to the medicine field. The invention also relates to application of Houttuynoid B in preparing the leukemia treatment medicine, application of Houttuynoid B in preparing leukemia cell proliferation inhibiting medicine, and application of Houttuynoid B in preparing medicine for inducing leukemia cell apoptosis. Houttuynoid B can treat leukemia by inhibiting leukemia cell proliferation and inducing leukemia cell apoptosis. The application of Houttuynoid B in preparing the leukemia treatment medicine, which is provided by the invention, is disclosed for the first time, and because the skeleton type belongs to brand-new skeleton type, the inhibiting activity of Houttuynoid B to leukemia cells is extremely strong.
EP1299381B1 Substituted quinazoline derivatives and their use as inhibitors The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C¿1-6?alkyl; R?5¿ is an optionally substituted 5-membered heteroaromatic ring, R?1, R2, R3, R4¿ are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed.
WO2004014842A8 Acylated arylcycloalkylamines and their use as pharmaceuticals The present invention relates to acylated arylcycloalkylamines of the formula I, in which R1, R2 and n have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds which are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (NO) synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
US20110281826 Stilbene derivatives for adp-ribosyl cyclase inhibitors The present disclosure relates to bisphenyl compounds that are useful for inhibiting the ADP-ribosyl cyclase (ADPR-cyclase). More particularly, the disclosed compounds can be used for treatment and prevention of hypertension, hypertensive cardiac hypertrophy, diabetes, and diabetic nephropathy, in which pathogenesis ADPR-cyclase is involved. The compounds and compositions of the invention can be used for treatment and prevention of cardiovascular disease and related disease states, particularly, hypertension or diabetes related disorders, such as, hypertensive cardiac hypertrophy, diabetic nephropathy, and the like.
EP1525201A1 Bicyclic piperidine derivatives as antagonists of the ccr1 chemokine receptor A compound of the formula (I) wherein a, b, cR1, R2, R3, R4, R5, R6, Q, W, Y, and Z are defined as above, useful as potent and selective inhibitors of MIP-1α(CCL3) binding to its receptor CCR1 found on inflammatory and immunomodulatory cells (preferably leukocytes and lymphocytes).
US20080200496 SUBSTITUTED 1H-PYRROLO[3,2-b, 3,2-c, and 2,3-c]PYRIDINE-2-CARBOXAMIDES AND RELATED ANALOGS AS INHIBITORS OF CASEIN KINASE Ie The present invention discloses and claims compounds of formula (I) wherein M is N, and K and L are each C with the remaining substituents further defined herein. These compounds are effective as inhibitors of human casein kinase Iε, and as such are useful in the treatment of central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.
US20110008476 Methods of Treating or Preventing Inflammatory Diseases of the Intestinal Tract The present invention relates to a glucan derived from yeast having a beta-(1, 3)-backbone with one or more beta-(1, 3)-side chains linked thereto for use in the treatment or prevention of inflammatory bowel disease and related diseases of abnormal bowel function in an animal, in particular to such uses employing a soluble glucan, e.g. from Saccharomyces cerevisiae, preferably when administered orally. The invention also relates to alternative treatments of inflammatory bowel disease and related diseases of abnormal bowel function utilising meal or protein derived from Asteraceae.
US20080081823 increase of the blood glucose level or decreasing the blood glucose level; enhancing insulin sensitivity or improving insulin resistance; antilipemic agents; use in foods, supplements, animal feeds; nontoxic The present invention discloses a composition containing a component that is an in vivo intrinsic substance and widely-consumed. The present invention provides a composition containing pipecolic acid in its provided amount of 20 mg/kg to 2000 mg/kg of body weight per day. The composition of the present invention can be used, for example, in the treatment of diabetes.
US6884773 Modified hemoglobins, including nitrosylhemoglobins, and uses thereof Diseases which can be ameliorated by delivery of NO to tissues affected by the disease can be treated by administration of nitrosyl-heme-containing donors of NO, including nitrosylhemoglobin. Nitrosylhemoglobin can be made by the reaction of NO with hemoglobin under certain conditions in which the NO:hemoglobin ratio is critical, and is converted to SNO-Hb under physiological conditions.
CN1872168A Compound spraying agent for rhinitis, and preparation method A medicine in the form of aerosol for treating rhinitis is prepared from ephedrine hydrochloride, benadryl hydrochloride, and the concentrated liquid extracts of green chiretta and small centripeda herb through dissolving in water, filtering, stirring, adding mint oil and eucalyptus oil, stirring, adding tween-80 (or span-80), adding water and stirring.
CN101069687A Entecavir dispersing tablet and preparing method The present invention discloses an anti-hepatitis B medicine enticavi dispersing tablet preparation and its preparation method. Said preparation adopts proper binding agent and prescription, and the invented enticavi dispersing tablet has high bioavailabity and blood concentration and good disintegration solution effect.
US20050014766 Use of n-(indolecarbonyl-)piperazine derivatives Use of compounds of the formula (I) in which R1, R4, R2, R4 and R5 are as defined in claim 1, and physiologically acceptable salts and solvates thereof, for the treatment of obesity, sub-types of anxiety, sub-types of schizophrenia and types of dementia of various origin.
US20110189312 Compositions and Methods for Supporting Heat Shock Protein Function Compositions and methods for promoting or maintaining protein accretion in cells, particularly in skeletal muscle cells, by supporting heat shock protein function. The compositions comprise glutamine and additional components directed at enhancing the activity of heat shock proteins.
US8580781 Pyridazinone derivatives Compounds of the formula (I), in which R1, R2, R3, R4, R4′ have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
EP2560644A1 A pharmaceutical composition comprising antiplatelet agents and an erythropoiesis stimulating agent The present invention is related to the composition comprising suitable antiplatelet agent/agents and the erythropoiesis stimulating agent for the treatment and improvement of kidney function. Further the present combination also provides the treatment and improvement in cardiovascular and bleeding related disorders. Specifically this composition shows synergistic interaction and significantly reduces the kidney damages caused by administrated erythropoiesis stimulating agents. Moreover the present composition normalizes the platelet reactivity and bleeding time in chronic kidney disease patient.
CN103638466A Medicine for treating cervical spondylosis and preparation method of medicine The invention discloses a medicine for treating cervical spondylosis and a preparation method of the medicine. The medicine is mainly prepared from radix angelicae pubescentis, ligusticum, turmeric, rhizoma cimicifugae, fructus viticis, gentiana macrophylla, pangolin, kudzuvine root and other medicines in a certain weight ratio. The medicine has the functions of nourishing blood and relaxing tendons, expelling wind and removing cold, removing dampness and relieving pain, and is quick in response and good in curative effect when used for treating cervical spondylosis, and does not have toxic or side effect.
US20100010078 Methods of treating androgen dependent prostate cancer by administering an active pharmaceutical ingredient being fisetin, 3,3',4',7-tetrahydroxyflavone or a derivative thereof, in an oral, transdermal or topical dosage form Administration of fisetin (3,3′,4′,7-tetrahydroxyflavone) to a human male to treat androgen dependent prostate cancer. Fisetin is found in fruits and vegetables, such as strawberry, apple, persimmon, grape, onion and cucumber. Fisetin treatment, through modulations in cki-cyclin-cdk network, inhibits PI3K and Akt resulting in inhibition of cell growth followed by apoptosis of human prostate cancer LNCaP cells.
US7416848 DNA encoding SNORF25 receptor This invention provides isolated nucleic acids encoding mammalian SNORF25 receptors, purified mammalian SNORF25 receptors, vectors comprising nucleic acid encoding mammalian SNORF25 receptors, cells comprising such vectors, antibodies directed to mammalian SNORF25 receptors, nucleic acid probes useful for detecting nucleic acid encoding mammalian SNORF25 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding mammalian SNORF25 receptors, transgenic, nonhuman animals which express DNA encoding normal or mutant mammalian SNORF25 receptors, methods of isolating mammalian SNORF25 receptors, methods of treating an abnormality that is linked to the activity of the mammalian SNORF25 receptors, as well as methods of determining binding of compounds to mammalian SNORF25 receptors, methods of identifying agonists and antagonists of SNORF25 receptors, and agonists and antagonists so identified.
WO2010079668A1 Olefin compound Disclosed is a compound represented by general formula (I) or a pharmacologically acceptable salt thereof. (In the formula, R1, R2, R2', R4, R5, R6, R7, R8 and R8' each represents a hydrogen atom or the like; and R3 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group or the like.)
US20130108694 Dry blend formulation of tetrahydrobiopterin Dry blend powder formulations comprising a pharmaceutical formulation containing tetrahydrobiopterin, and methods of making and using the same, are disclosed herein.
CN103142565A Novel nimesulide sustained-release pharmaceutical composition and preparation method thereof The invention discloses a novel nimesulide sustained-release pharmaceutical composition and a preparation method thereof. The novel nimesulide sustained-release pharmaceutical composition contains nimesulide as an active component, an alkalizer and any pharmaceutically acceptable auxiliary materials. The novel nimesulide sustained-release pharmaceutical composition has the advantages of simple formula, easy operation, stable quality, strong controllability and good reappearance.
US6924279 An antibiotics for treating bacterial infections; bactericides This invention provides crystalline forms of a 1-methylcarbapenem derivative of formula (I) or of pharmaceutically acceptable salts thereof. The crystalline forms of the 1-methylcarbapenem derivative exhibit excellent antibiotic activity against various bacterial strains and sufficient stability for practical use.
CN102451214A Medicament for human skin The invention relates to a medicament for human skin, which is prepared from 50 percent of dexamethasone, 10 percent of calamine, 15 percent of vitamin B6, 15 percent of gold-threaded calabash and 10 percent of cocklebur fruit. A preparation method of the medicament comprises the following steps of: (1) juicing 15g of gold-threaded calabash stem leaves to obtain a solution 1; (2) juicing 10g of cocklebur fruit stem leaves to obtain a solution 2; (3) mixing the solution 1 and the solution 2 to obtain a solution 3; and (4) adding 50g of dexamethasone, 10g of calamine and 15g of vitamin B6 to the obtained solution 3, and evenly stirring until the liquid is sticky to obtain the medicament. The medicament for human skin, disclosed by the invention, has the beneficial effects of favorable curative effect to intractable tinea symptoms and no irritation.
US20120095004 Sphingosine Kinase Inhibitors The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
CN101933934A Novel application of ginsenoside Rb1 The invention discloses application of ginsenoside Rb1 to preparing a medicament for treating myocardial ischemia and also discloses application thereof to preparing medicaments for lowering heart rate and fighting hypoxia when myocardial ischemia is treated. Through experiments, the applications are proved to have important clinical meanings.
CN102008539A Medicinal composition for treating diseases such as vital myocarditis and dilated cardiomyopathy and preparation process thereof The invention relates to a medicinal composition for treating diseases such as vital myocarditis and dilated cardiomyopathy. The composition is prepared from the following raw material medicaments in part by weight: 10 to 200 parts of pseudoginseng root, 20 to 300 parts of American ginseng, 15 to 60 parts of frank incense, 15 to 60 parts of myrrh, 15 to 80 parts of ground beetle, 20 to 60 parts of dragon bone, 15 to 30 parts of native copper, 2 to 5 parts of musk, 15 to 300 parts of rhodiola, 15 to 60 parts of rosewood and 5 to 10 parts of borneol. Meanwhile, the invention also discloses a preparation process of the composition. By the preparation process, methods such as expelling stasis, promoting tissue regeneration and freeing network vessels and the like for treating the vital myocarditis are combined with methods such as tonifying vitality, activating blood and dissolving stasis for treating dilated myocarditis, so that myocardial cells can be promoted to be regenerated, the vitality of the myocardial cells is comprehensively recovered and improved, the functions of dysfunctional myocardial cells are promoted to be recovered, and the conditions of inhibiting cell apoptosis, promoting the recovery of the myocardial cells and the like are improved to a certain extent.
US20080293719 Pyridiazinone Derivatives for the Treatment of Tumours Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours
CN102807576A Novel fat-soluble binuclear Cu (II) anticancer complex The invention relates to a fat-soluble binuclear Cu (II) anticancer complex, namely N,N'-bis(salicylaldehyde) diamine copper (II). The N,N'-bis(salicylaldehyde) diamine copper (II) is prepared by carrying out quantitative reaction on CuAc2 4H2O as a raw material and a ligand N,N'-(salicylaldehyde) dazine in a DMF (Dimethyl Formamide) solvent to separate out a reddish-brown crystal of the fat-soluble binuclear Cu (II) anticancer complex disclosed by the invention. The fat-soluble binuclear Cu (II) anticancer complex disclosed by the invention has favorable anticancer activity superior to cis-platinum and carboplatin and favorable fat solubility and is used for clinically treating cancer.
CN102008447A Entecavir solid dispersion and preparation thereof The invention relates to an entecavir solid dispersion and a preparation containing the entecavir solid dispersion. The entecavir solid dispersion of the invention is mainly prepared from an effective quantity of entecavir, a carrier and Tween-80, and the carrier can be polyethylene glycol and/or poloxamer. The entecavir solid dispersion of the invention has high dissolution rate in water, and the bioavailability of entecavir can be improved.
US20100151021 Compositions Comprising Melperone The present invention is directed to pharmaceutical compositions, and methods of making such compositions, comprising microparticles containing melperone and/or a pharmaceutically acceptable salt, solvate, or ester thereof; a layer of alkaline buffer, and a controlled-release coating. The present invention is also directed to pharmaceutical dosage forms, including orally disintegrating tablets, conventional tablets, and capsules, and methods for their preparation.
US20080233595 Method for diagnosing intertility The invention relates to methods for diagnosing conditions characterized by altered expression of a pregnancy related serine protease (PRSP) protein in a mammal. Such conditions include infertility caused by an inability to achieve or sustain embryo implantation, an inability to sustain a pregnancy, early abortion, insufficient placentation, pre-eclampsia, or intrauterine growth restriction. The methods include detecting expression of PRSP, such as SEQ ID NP33. Detection may be accomplished using a PRSP-specific antibody.
CN101669898A Medicinal preparation for injective administration and preparation method thereof The invention provides a medicinal preparation for injective administration and a preparation method thereof. The medicinal preparation comprises anastrozole and solubilizer, and has the advantages that: (1) the preparation successfully solves the technical problem that the anastrozole is insoluble in water and is not suitable to be prepared into injection in the prior art, and greatly improves the bioavailability of the anastrozole while overcoming the defect that anastrozole tablets irritate gastrointestinal tract, so that the preparation is more effective for treating woman advanced breastcancer; (2) the medicinal preparation has stable property and non pollution to light, heat, oxygen, water and the like, is convenient for preparation, transportation and storage, and is suitable for mass production; (3) freeze-dried powder injection solves the problem of transportation and storage in winter in northern and severe cold areas, reduces volume and weight of products with the same dosage and greatly reduces transportation cost in an operating process; and (4) the injection and infusion can effectively prevent pollution in a dispensing process.
EP1507527A2 Methods for enhancing motor performance and/or endurance The present invention provides methods for enhancing muscle performance and/or endurance by administering a composition comprising a desmethyl tocopherol. Athletic performance and sports medicine in general are benefited by the methods of the invention. In addition, the invention provides the therapeutic utility to muscle disorders that involve nitrative stress and/or inflammation.
US20090197897 Novel Oxadiazole Derivatives and Their Use as Positive Allosteric Modulators of Metabotropic Glutamate Receptors The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or peripheral nervous system disorders as well as other disorders modulated by mGluR5 receptors.
WO2014049063A1 Formulations involving solvent/detergent-treated plasma (s/d plasma) and uses thereof The invention concerns pharmaceutical formulations comprising solvent/detergent (S/D)-treated plasma and a glycosaminoglycan such as hyaluronic acid, and their use for treating diseases, particularly musculoskeletal diseases.
EP1705177A1 N-aryl-sulfoximine-substituted pyrimidines as CDK- and/or VEGF inhibitors, their production and use as pharmaceutical agents This invention relates to pyrimidine derivatives of general formula (I) in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.
US20090105191 Pharmaceutical and Dermatocosmetic Compositions Comprising Extract of Durio Zibenthinus The present invention relates to dermatocosmetic and pharmaceutical compositions comprising compounds obtained from Durio zibethinus and their use in increasing phase angle and reducing the signs and appearance of photoaging and biological aging.
WO2013148824A1 METHODS AND COMPOSITIONS TO TREAT CANCER USING BIFUNCTIONAL SRC-3 shRNA The present invention includes compositions and methods of making and using an expression vector comprising a promoter and a nucleic acid insert operably linked to the promoter, wherein the insert encodes one or more short hairpin RNAs (shRNA) capable of inhibiting an expression of a SRC-3 gene via RNA interference, wherein the one or more shRNA comprise a bifunctional RNA molecule that activates a cleavage-dependent and a cleavage-independent RNA-induced silencing complex for reducing the expression level of the SRC-3.
US7410641 Hybridoma and monoclonal antibodies produced; insulin-like growth factor (IGF); diagnosis, treatment, prevention of diabetes and metabolic disorders The present invention relates to antibodies that bind to the A chain N-terminal peptide. The present invention also relates to (1) a polypeptide containing the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO:7 (A chain), (2) a polypeptide containing the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO:8 (B chain), (3) a polypeptide wherein the A and B chains are bonded to each other via disulfide bonds (2 chains) or its salt., (4) DNAs encoding the same, etc. These polypeptides and DNAs encoding the same can be used for the diagnosis, treatment, prevention, etc. for diseases, including abnormalities (e.g., diabetes mellitus, etc.) in metabolic regulation (sugar metabolism, lipid metabolism, etc.) of energy sources such as carbohydrates.
WO2014126267A1 Difluprednate emulsion composition containing antimicrobial metal The present invention provides a difluprednate emulsion composition showing immediate effectiveness of preservative efficacy. The immediate effectiveness of preservative efficacy is achieved by adding an antimicrobial metal (excluding zinc). The present invention also provides a method of conferring immediate effectiveness of the preservative efficacy to an emulsion composition comprising difluprednate, the method includes preparing an emulsion composition comprising difluprednate and an antimicrobial metal (excluding zinc).
US20110020231 Quaternary ammonium diphenylmethyl compounds useful as muscarinic receptor antagonists The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
US20070244086 3-Phenyl-Pyrazole Derivatives as Modulators of the 5-Ht2A Serotonin Receptor Useful for the Treatment of Disorders Related Thereto The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
WO2011047173A9 Pharmaceutical compositions for oral administration This invention is directed to pharmaceutical compositions for oral administration to a mammal, wherein the pharmaceutical compositions comprise a spiro-oxindole compound, as a single stereoisomer or as a mixture thereof, or a pharmaceutically acceptable salt thereof. These pharmaceutical compositions are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
CN1955170B Class I tanshinone II A derivative and its application in pharmacy This invention relates to a category of tanshinone IIA derivate, this derivate connects with saturated fatty acid or unsaturated fatty acid at alpha-position of furan ring of tanshinone IIA, structural formula is formula I, among them, X is -(CHR)n-COOH,R=H or alkyl group whose carbon number is 1-8, n=0-8;or is -(CR=CH)n-COOH,R=H or alkyl group of which carbon number is 1-8, n=0-4. This tanshinone IIA derivate provides a dependable way for clinical application of tanshinone IIA, redeem the defect that acidity is excessively strong, stimulation is large, which is caused by sulfonic acid natrium injection of tanshinone IIA that is used as clinical medicine.
US20080075713 isomerase enzymes and ATP-binding cassette (ABC) transport proteins, used for controlling metabolism of triglycerides; diagnosis, prevention and treatment of metabolic disorders The present invention discloses three novel proteins regulating the energy homeostasis and the metabolism of triglycerides, and polynucleotides, which identify and encode the proteins disclosed in this invention. The invention also relates to vectors, host cells, antibodies, and recombinant methods for producing the polypeptides and polynucleotides of the invention. The invention also relates to the use of these sequences in the diagnosis, study, prevention, and treatment of diseases and disorders related to body-weight regulation, for example, but not limited to, metabolic diseases such as obesity, as well as related disorders such as adipositas, eating disorders, wasting syndromes (cachexia), pancreatic dysfunctions (such as diabetes mellitus), hypertension., pancreatic dysfunctions, arteriosclerosis, coronary artery disease (CAD), coronary heart disease, hypercholesterolemia, dyslipidemia, osteoarthritis, gallstones, cancer, e.g. cancers of the reproductive organs, sleep apnea, and others.
WO2012149566A3 Anti-hiv group i introns and a uses thereof in treating hiv infections Described is a unique class of antiviral molecule that can be applied to control and eliminate HIV infection in patients using myeloablation therapies and replenishment with transformed bone marrow stem cells programmed to express the antiviral molecule. These anti-viral molecules target the HIV genome in a highly conserved domain, and when expressed in cells prior to infection will cause the cell to die upon infection with HIV. Cell death insures no proliferation of new virus. Reconstituting the immune system with cells expressing these antivirals prevents re-establishment of HIV infection from reservoirs in the re-established lymphocyte and macrophage populations. Over time, reservoirs will be depleted entirely, effectively eliminating the virus. In effect, this new type of antiviral can be used to cure HIV infections.
US20070293503 Phenylenediamine urotensin-II receptor antagonists and CCR-9 antagonists The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
CN103417669A Drug for treatment of abdominal pain and diarrhea The invention discloses drug for the treatment of abdominal pain and diarrhea and belongs to the field of TCM. The drug comprises pharmaceutical effective ingredients, including Chinese granesbill, turtle shell, Eryngium foetidum herb, multibract raspberry root, cutch, birch bark, radish seed, Asiatic pennywort herb, common turczaninowia herb, Russian olive fruit, purple flower holly leaf, coastal heritiera seed, chalk, cucubalus root, Yunnan Pistache leaf, and quince. The drug has the effects of regulating qi to alleviate pain, clearing away heat and eliminating dampness, soothing the liver to dispel melancholy and tonifying the spleen to cure diarrhea, and has the significant effect of the diarrhea, watery stool, abdominal pain and poor appetite caused by damp-heat accumulation and the viral enteritis and non-infectious diarrhea caused by rotavirus. The drug has the advantages that the preparation process is simple, curative effect is good and fast, the drug is convenient to take and available for treating both symptoms and root causes, and the drug is neutral in property and has no toxic and side effects; the drug has good effects for the treatment of inappetence, nausea and vomiting, abdominal distension and diarrhea, and dyspepsia.
WO2013103668A1 Formulations for enhanced bioavailability of zanamivir In accordance with the present invention, there are provided compositions comprising zanamivir and at least one permeability enhancer. The compositions can increase the amount of zanamivir capable of being transported across a cell membrane (such as a Caco-2 cell membrane), and can increase this amount by at least 150% relative to the amount capable of being transported across the cell membrane in the absence of the permeability enhancer. Also provided are oral dosage forms of the compositions, which comprise a therapeutically effective amount of zanamivir and a permeability-enhancing amount of a permeability enhancer. The oral dosage forms can further comprise an enteric- or pH-sensitive coating or layer surrounding the composition. Also provided in accordance with the present invention are methods for treating or preventing influenza infection.
US20080033057 Hexahydro-isoalpha acid based protein kinase modulation cancer treatment Compounds and methods for protein kinase modulation for cancer treatment are disclosed. The compounds and methods disclosed are based on hexahydro-isoalpha acids, commonly found in hops.
EP2681206A1 Mst1 kinase inhibitors and methods of their use Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders. Particular compounds are of the formula:
EP1575982A1 Promoter for the production of hyaluronic acid containing ginsenoside compound k There are provided a promoter containing ginsenoside compound K for the production of hyaluronic acid, and more particularly, a new efficacy of 20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol (compound K), a chief metabolite of ginseng saponin, to increase the expression of hyaluronic acid synthase gene in human cell and thereby to promote the production of hyaluronic acid, and an anti-aging agent containing the promoter for the production of hyaluronic acid as an effective ingredient.
CN101849931A Medicament for treating encephalatrophy or encephalatrophic dementia The invention relates to new medical application of theanine, in particular to application of the theanine in preparing a medicament or health-care product for treating the encephalatrophy or encephalatrophic dementia, and belongs to the field of medicaments or health-care products. At present, a few medicaments for treating the encephalatrophy or encephalatrophic dementia are available and the therapeutic effect is not obvious. The theanine serving as the medicament for treating the encephalatrophy or encephalatrophic dementia has the advantages of obvious therapeutic effect, readily available raw materials and realization of industrial production by using conventional normal pharmaceutical equipment.
CN103327983A Dosage and administration for preventing cardiotoxicity in treatment with ERBB2-targeted immunoliposomes comprising anthracyclin chemotherapeutic agents Methods for determining dosage of HER2-targeted anthracycline-containing immunoliposomes are disclosed, as are methods of treating cancer patients with HER2-positive tumors using dosages so determined. Upon administration, the dosages share the low cardiotoxicity profile of standard dosages of non-immunoliposomal (untargeted), anthracycline-containing liposomes.
WO2013078446A3 Derivatives of phenoxyisobutyric acid The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
CN101347539A Medicament for treating ache of joint and preparation thereof The invention discloses a medicine for treating arthralgia and a preparation method thereof and relates to a medicine for treating ache and a preparation method thereof. The medicine of the invention solves the problem that oral administration in the existing medicines for treating arthralgia have poor pertinence and ache is likely to relapse after withdrawal of external medicines. The medicine of the invention for treating arthralgia is essentially prepared by zanthoxylum micranthum, rhizoma corydalis, artificial musk, frankincense, myrrh, menthol and methyl salicylate; the preparation method includes the following steps: ethanol within the temperature of 55-65 DEG C and with volume concentration of 90 % is used for soaking the medicinal materials; after filtration, filtrate is merged, added with other excipients and menthol, and then is added with ethanol to a fixed amount to obtain the medicine for treating arthralgia; the medicine of the invention has good curative effect on the arthralgia caused by various reasons, and arthralgia does not relapse after withdrawal of the medicine.
CN102499986A Macromolecule-cis-platinum compound, preparation method and application thereof The invention relates to a macromolecule-cis-platinum compound, a preparation method and application thereof. The preparation method comprises the following steps of: degrading or purifying polyamino acid serving as a raw material to obtain a polyamino acid carrier with appropriate molecular weight; performing reaction of a small molecular acid serving as a modifier and side chain active groups of the small molecular acid, modifying a structure of the small molecular acid, and connecting cis-platinum to the polymer skillfully to prepare the medicine-carrying compound. The result of the study on the properties of the medicine-carrying compound indicates that the properties of the medicine-carrying compound are obviously superior to the conventional report, and the prepared compound is low in toxicity and does not have hemolysis.
CN101502485A Nano cubic liquid crystal dexamethasone preparation for eye and preparation method thereof The invention relates to a dexamethasone ophthalmic nano-cubic liquid-crystal preparation and a preparation method thereof. The dexamethasone ophthalmic nanocube crystal preparation is prepared from lipid materials, an emulsifying agent, a thickening agent, an osmotic pressure regulating agent, a bacteriostatic agent, a pH value regulating agent and purified water and characterized in that the amphipathic lipid capable of forming the cubic liquid-crystal morphology, one or more out of glyceryl monooleate (GMO), phytantriol and lecithin are adopted as the lipid materials; and the safe and non-irritant ophthalmic surfactant, one or more out of poloxamer 407 and polyvinyl alcohol (PVA) are adopted as the emulsifying agent. .The invention realizes the ophthalmic administration of dexamethasone, a fat-soluble drug, and has the advantages of high comfort level and non-irritant administration; and the invention can promote the drug to permeate into the corneal barriers after the ophthalmic administration, thereby achieving the effect of improving the ophthalmic bioavailability.
CA2436361C Angiotensin ii antagonistic compound for use as analgesic and antiinflammatory agent Excellent analgesic and antiinflammatory agents comprising a compound having an angiotensin II antagonistic activity, its prodrugs thereof or salts of the same.
WO2011109743A3 Synergistic effects of combinations of buprenorphine and opioids for the treatment of pain Disclosed herein are compositions and methods for treating pain, and addiction, said methods comprising administering: at least one Opioid or a pharmaceutically acceptable salt thereof; and at least one of a μ- receptor partial agonist or a κ-receptor antagonist, or pharmaceutically acceptable salts thereof; in amounts effective to cause or enhance a supra-additive synergistic analgesic response to pain and for a duration effective to inhibit pain in the individual in need thereof. The co-administration of an Opioid with the μ-receptor partial agonist and the κ-receptor antagonist results in decreased tolerance, decreased dependence potential, and diminishing side effects, compared to conventional opioid therapy alone.
US20080138437 Reduce toxicity while maintaining efficacy; mix with particulate hydroxyapatite as an auxiliary agent; alkylating agent, antimetabolite, an antitumor antibiotic, plant preparation, hormone preparation, immunotherapeutic agent, cisplatin; injection, infusion, oral administration Due to the toxicity of antitumor agents, use of antitumor agents is limited, and thus, it is desirable to develop auxiliary agents or antitumor agents that have the effect of reducing toxicity while maintaining the antitumor effect of antitumor agents. The present invention provides antitumor agents mixed with particulate hydroxyapatite as an auxiliary agent.
US20110130379 Piperazine derivatives used as cav2.2 calcium channel modulators The present invention relates to novel piperazine derivatives (I); to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
US7063864 Morphine sulphate microgranules, method for preparing same and compositions containing same The present invention concerns a novel sustained-release oral formulation of morphine sulphate in the form of microgranules. Each microgranule comprises a neutral support grain coated with an active layer and with a sustained-release layer, characterized in that the sustained-release layer contains a copolymer of methacrylic acid and of methyl methacrylate ester, the relative proportion of the free carboxyl groups and of the ester groups of which is equal to 0.5 approximately, and a silica exhibiting a hydrophobic character. The present invention also concerns a process for preparing these microgranules which is carried out entirely in aqueous medium by emplacing on neutral support grains.
WO2008096021A3 Process for continuous production of lovastatine Process for continuous production of lovastatine. The present invention consists of the production of lovastatine, from cultures of Aspergillus terreus in the form of pellets, by means of a continuous fermentation process in a bubble column bioreactor operating in a similar way to a fluidized bed bioreactor (BLF) with a culture in three steps, gas, liquid and solid. Lovastatine production is regulated by means of a product inhibition mechanism, thereby halting synthesis when the concentration reaches a predetermined value. The process provides continuous production of a biomass-free fermentation medium containing the lovastine, thereby facilitating the subsequent steps of extraction and purification. The continuous operation causes part of the lovastatine generated to come out of the fluidized bed bioreactor, thereby lessening the effects of product inhibition.
US20100093653 Use of 1,6-Bis [3-(3-carboxymethylphenyl)-4-(2-alpha-D-mannopyranosyl-oxy)-phenyl] hexane for the preparation of cosmetic compositions A compound of formula (I) or a polymorphic form thereof can be used for the preparation of a cosmetic or dermato logical composition for the treatment of skin ageing.
EP2464333A2 Floating microgranules The present invention relates to a floating granule containing a solid core whereon an active principle is mounted. Said floating granule also contains a compound capable of generating a gas evolution consisting of an alkaline agent.
US7528134 Acetamides and benzamides that are useful in treating sexual dysfunction The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
US20090074753 Platelet-derived growth factor compositions and methods of use thereof A method for promoting growth of bone, periodontium, ligament, or cartilage in a mammal by applying to the bone, periodontium, ligament, or cartilage a composition comprising platelet-derived growth factor at a concentration in the range of about 0.1 mg/mL to about 1.0 mg/mL in a pharmaceutically acceptable liquid carrier and a pharmaceutically-acceptable solid carrier.
EP1526847A2 Pharmaceutical dosage form comprising a sulfite compound The present invention provides a pharmaceutical dosage form comprising a fill material sealed in a gelatin capsule; the fill material comprises (a) a selective COX-2 inhibitory drug of low water solubility, and (b) a sulfite compound in an amount sufficient to inhibit cross-linking of gelatin in said gelatin capsule upon storage of the dosage form in a closed container maintained at 40°C and 75% relative humidity for a period of 6 months.
US20090148489 Bioabsorbable material A bioabsorbable material suitable for implanting within a human body, the material including fibers of a composite of a synthetic bioabsorbable polymer such as poly-lactic acid, and a particulate bioactive filler such as calcium phosphate powder. The fibers are discontinuous with non-uniform cross-sections and non-uniform cross-sectional areas. The surface topography provided by the fibers provides a substrate which is more amenable to cellular colonization than prior materials.
CN101423517B Gamma-carbolines derivates as well as preparation method and application thereof The invention provides a gamma-carboline derivative, which is obtained by using gamma-carboline with antineoplastic activity as a lead compound, and introducing different lateral chains, aromatic rings, aromatic heterocycles or heterocycles to the sixth position of the gamma-carboline. Pharmacological active screening test shows that the compound has in-vitro antihyperplasia function on tumor cells; partial compound has obvious anti-tumor activity; the value of IC50 reaches mu M grade to show cytotoxicity similar to positive control polyenic taxusol; and significant microtubulin polymerization retardation activity and DNA intercalation function are presented in primary activity mechanism research; therefore, the compound is expected to be a new antineoplastic reagent with double functions of micromolecular microtubulin and DNA. The gamma-carboline derivative has the advantages of reasonable design, wide source of raw materials, easy preparation, mild reaction condition, simple operation and practicality. The structural formula of the compound is shown as the above.
WO2013124807A3 Oligonucleotides for modulating gene expression and uses thereof The present invention regards oligonucleotides for modulating the expression of a gene, in particular for modulating a gene responsible for a pathology of genetic, tumoural or viral origin. Moreover, the present invention relates to the use of said oligonucleotides, possibly chemically modified, for the treatment and/or the diagnosis of said diseases.
WO2011073155A1 Novel antagonists for ccr2 and uses thereof The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
CN102429920A Multi-associative hematic acid reducing composition and preparation method thereof The invention discloses a multi-associative hematic acid reducing composition and a preparation method thereof. The multi-associative hematic acid reducing composition disclosed by the invention consists of lycine, vitamins and trace elements serving as major raw materials. The multi-associative hematic acid reducing composition disclosed by the invention can be used for reducing the content of high homocysteine in the blood of a human body and replenishing total methyl nutrients necessary for the protein metabolism process of the human body in time, so that the human body is in the optimal nutritional state, and the potential health risk is switched to the healthy state to the maximum extent.
CN100998673B Compound cream containing fluconazole and Radix scutellariae and its preparing method A fluconazole-scutellaria cream for treating dermatitis, eczema, ringworm of body, tinea manuum, tinea pedis, itching, etc is prepared proportionally from fluconazole, neomycin sulfate, prednisone acetate, the extracts of scutellaria root and dittany bark, and O/W-type cream matrix. Its preparing process is also disclosed.
CN1748704B Aqueous preparation for injection and its stabilizing method 5-formoxyl-(6s)-tetrahydrofolic acid or the acceptable salt in the pharmacology which is used for strengthening the antineoplastic effect of fluorouracil to gastric cancer and colon and rectum cancer is unstable and can not be kept for a long time when prepared as water solution. As a result, only solid form preparation of the 5-formoxyl-(6s)-tetrahydrofolic acid or the acceptable salt in the pharmacology is developed and available on the market. However, clinically, the development of stable injection water solution preparation of the 5-formoxyl-(6s)-tetrahydrofolic acid or the acceptable salt in the pharmacology, which can be used directly for dosing, is required. The invention provides a stable injection water solution preparation of 5-formoxyl-(6s)-tetrahydrofolic acid or the acceptable salt in the pharmacology and a method for stabilizing the 5-formoxyl-(6s)-tetrahydrofolic acid or the acceptable salt in the pharmacology. The preparation of the invention using a PH regulator and an antioxidant shows excellent effect of storage stability.
US20110178142 Pharmaceutical composition for therapeutic or prophylactic treatment of bacterial infections and associated diseases The present invention provides a pharmaceutical composition comprising 3-{5-[4-Oxo-2-thioxo-3-(3-trifluoromethyl-phenyl)-thiazolidin-5-ylidenemethyl]-furan-2-yl}-benzoic acid or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable excipients for therapeutic or prophylactic treatment of bacterial infections and diseases associated thereof.
WO2010011857A2 Parenteral administration of a glucosamine Materials and methods for local delivery of a glucosamine are provided to facilitate bone and cartilage growth.
US7456214 Cancer; for selectively destroying tumor vasculature; inhibit tubulin polymerization; selectively reducing blood flow to at least a portion of a neoplastic region; 3-(3',4',5'-Trimethoxybenzoyl)-6-hydroxy-7-methoxy-2H-chromene Chrome compounds have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.
US20090062214 Left-Side Glucose Lipid a Analogue A compound having excellent macrophage activity inhibitory action, which is represented by the general following formula: wherein Q represents an oxygen atom, a C1-C3 alkylene group, a —O-Alk- group or a —O-Alk-O— group (in which Alk is a C1-C3 alkylene group), R1 represents a C1-C20 alkanoyl group which may be substituted, a C3-C20 alkenoyl group which may be substituted or a C3-C20 alkynoyl group which may be substituted, R2, R3 and R4, which may be the same or different, represent a hydrogen atom, a C1-C20 alkyl group which may be substituted, a C2-C20 alkenyl group which may be substituted, a C2-C20 alkynyl group which may be substituted, a C1-C20 alkanoyl group which may be substituted, a C3-C20 alkenoyl group which may be substituted or a C3-C20 alkynoyl group which may be substituted, R5 represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-C6 alkoxy group which may be substituted, a C2-C6 alkenyloxy group which may be substituted or a C2-C6 alkynyloxy group which may be substituted, and W represents an oxygen atom or a —NH— group, or a pharmacologically acceptable salt thereof.
EP1886690A2 Pharmaceutical composition for the treatment of food intolerance Composition (A), preferably in the form of a pharmaceutical preparation, for preventing and/or treating food indigestion, preferably food indigestion with stomach/intestinal complaints, comprises Okoubaka (0.1-50 wt.%), 3,3',4',5,7-pentahydroxyflavone (0.1-40 wt.%), at least a galactosidase (0.0001-10 wt.%) and pyridoxine, preferably pyridoxine hydrochloride (vitamin B6) (0.001-10 wt.%). - ACTIVITY : Metabolic; Gastrointestinal-gen.; Analgesic; Antiemetic; Antiflatulent; Antidiarrheic. - MECHANISM OF ACTION : None given.
CN103214543A New maslinic acid derivatives, preparation method, and applications of new maslinic acid derivative in antitumor drug The invention belongs to the field of nature pharmaceutical chemistry, and relates to preparation of two new compounds (1 and 2) represented by a chemical structure general formula (1). The present invention further relates to applications of the new compounds in antitumor drug preparation. The preparation method comprises: adopting screened syncephalastrum racemosum bacterial having structure modification ability to maslinic acid, carrying out fermentation culture under optimized conditions, carrying out conversion on maslinic acid for 7-10 days, extracting the converted product with an organic solvent, and carrying out separation and purification to obtain the two new maslinic acid derivatives.
CN103432080A Displayable drug-loaded nano silver sodium alginate microsphere blood vessel embolic agent and preparation method thereof The invention provides a displayable drug-loaded nano silver sodium alginate microsphere blood vessel embolic agent and a preparation method thereof, and relates to a blood vessel embolic agent and a preparation method thereof. An object of the invention is to solve the technical problems that a conventional drug-loaded sodium alginate microsphere blood vessel embolic agent has no X-ray visibility. The method comprises the steps of mixing a sodium alginate solution containing nano silver particles and an antineoplastic drug solution, mixing the above mixture with a solidifying liquid via a dropping method, and thus the displayable drug-loaded nano silver sodium alginate microsphere blood vessel embolic agent is obtained. The displayable drug-loaded nano silver sodium alginate microsphere blood vessel embolic agent has good visibility under X rays, is convenient for observing embolic degree, effectively prevents mistaken embolism, and at the same time, facilitates follow-up observation.
CN101559138B Externally applied medicament for treating porcine foot-and-mouth disease and PRRS The invention relates to an externally applied medicament for treating porcine foot-and-mouth disease and PRRS, which is processed and confected by the bulk drugs with parts by weight as follows: 2-3 parts of dried rhizome of rehmannia, 2-3 parts of Flos Daturae, 1-2 parts of borneol and 0.5-1 part of snake skin. The optimal matching proposal of the invention is as below: 2 parts of dried rhizomeof rehmannia, 2 parts of Flos Daturae, 1 part of borneol and 0.5 part of snake skin. The confecting method comprises the steps of weighing the bulk drugs according to the above parts by weight, grinding the bulk drugs, soaking the ground bulk drugs in liquor with alcoholicity above 56 degrees for 30-40 days, filtering the liquor and removing residues to prepare medicinal liquor. The medicinal liquor is sprayed or rubbed for 5-6 times every day and 7-day is a course of treatment. The drugs of the invention are reasonable in compatibility, address both the symptoms and root causes, are relevant to pathogenesis and have special effects, thus obtaining satisfactory treatment effects. The medicament features abundant drug sources, simple preparation method, low price, convenient use and no toxic side effects.
US20110003887 Treating oncogenic ras driven cancers Oncogenic Ras-driven cancer is treated with agent by interrupting pathway comprising activation of Akt by oncogenic Ras, activated Akt causing phosphorylation of eNOS at S1177 site of eNOS to provide activated eNOS in cancer cells and activated eNOS causing activation of wildtype Ras by nitrosylation thereof at C118 to provide GTP-bound activated wildtype H and N Ras. L-NAME can be orally administered to interrupt this pathway. Wortmannin can be administered intravenously to interrupt this pathway. Novel siRNAs are disclosed useful to interrupt said pathway.
EP1864673A2 Method for producing an anti-cancer agent A method for producing an anti-cancer agent based on coordination compounds of platinum (II), under which an aqueous solution containing humic acids is treated with the said platinum compound. The coordination compound of platinum is selected from the following range: potassium tetrachloroplatinate, cis-dichlorodiammineplatinum, hydrogen tetrachloroplatinate, potassium tetrabromoplatinate. The treatment is conducted under irradiation with waves until the concentration of the high molecular fraction of humic substances is brought to a level of 5% or less. The wave radiation is selected from the ultrasonic range, with frequencies from 18 kHz to 66 kHz and power density from 0.5 to 4 W/cm3. For 5 W/cm3 irradiation at the frequency of 22 kHz, the treatment is conducted for 5 to 20 minutes. Irradiation may also be performed with microwaves in the frequency range from 0.3 to 30 GHz and power from 0.5 to 50 kW. For 5 W/cm3 irradiation at the frequency of 2.45 GHz, the product being treated is maintained at the temperature of 60-70°C for 30 to 90 minutes.
US20120214758 Tyrosine kinase receptor antagonists and methods of treatment for pancreatic cancer A method of treatment is disclosed whereby cancer cells are brought into contact with a formulation comprising an inhibitor of tyrosine kinase receptors. The formulation may be comprised of an injectable carrier and two or more tyrosine kinase receptor inhibitors which may be nordihydrogluaiaretic acid (NDGA) and doxyrubicine.
CN101897665A Method for preparing diammonium glycyrrhizinate injection The invention discloses a method for preparing diammonium glycyrrhizinate injection, which comprises the following steps of: a, adding diammonium glycyrrhizinate into water for injection at the temperature of between 30 and 50 DEG C under the aseptic condition, and stirring to dissolve; b, regulating the pH value to be between 6.2 and 7.8 by using solution of sodium bicarbonate, and compensating the volume of the water for injection; c, adding active carbon for a needle accounting for 0.2 volume percent of the liquid medicament, stirring for 30 minutes, and decoloring and removing pyrogen; and d, coarsely filtering and decarbonizing the liquid medicament, disinfecting and filtering through a double-stage microfiltration membrane with the diameter of 0.22 mu m, packaging, and sterilizing by flowing steam for 30 minutes at the temperature of 121 DEG C. The method has the advantages of simple, convenient and practicable operation and convenient industrialized mass production. The diammonium glycyrrhizinate injection prepared by the method has product quality stability and product yield better than those of the products prepared in the prior art.
WO2006108225A1 Method of screening for compounds that modulate cell proliferation The invention provides a method of screening for compounds that modulate cell proliferation involving analysing the activity or expression of cortactin in the presence of a candidate compound wherein altered activity or expression of cortactin when compared to the absence of the compound indicates a potential modulator of cell proliferation. The invention also provides compounds identified by these methods, methods of reducing or enhancing cell proliferation in subjects in need thereof and methods for prognostic and diagnostic evaluation of diseases associated with aberrant cell proliferation.
CN1762345A Silybinin injection and its preparation method The invention relates to a silybin injection and its preparation method, which comprises silybin meglumine, glucosamine, alkaline amino acid solubiliser and pharmaceutically acceptable solvent, or compound of silybin and alkaline solubiliser and pharmaceutically acceptable solvent, the pH is 4-11. The injection also comprises one or more of pharmaceutically acceptable solubilizer, pH regulator, isotonic conditioning agent, painkiller, anti-oxidant agent, preservative and complexing agent.
CN103006545A Tiamulin alkali ointment and preparation method thereof The invention discloses a tiamulin alkali ointment and a preparation method thereof. The tiamulin alkali ointment comprises the following components in percentage by weight:75-85% of tiamulin, 0.8-1.4% of propylgallate, 1.2-1.8% of butylparaben and the balance of solvent. The invention provides a liquid tiamulin alkali ointment and provides a new option for the tiamulin crude drug. The ointment preparation process disclosed by the invention is simple; compared with the preparation method of tiamulin fumarate powder crude drug, the steps of salifying, crystallizing, drying, breaking and the like are omitted, so that the working efficiency is greatly enhanced, the labor strength is reduced and the production cost is reduced; after the special auxiliary material is added into the product, the safety and effectiveness are well guaranteed; and the preparation method disclosed by the invention is more suitable for industrialized mass production.
CA2335328C A substituted triazolo-pyridazine derivative, pharmaceutical compositions made therefrom 7- (1, 1-Dimethylethyl)-6-(2-ethyl- 2H- 1, 2, 4- triazol- 3-ylmethoxy) -3- (2-fluorophenyl) - 1,2,4-triazolo[4,3-b]pyridazine, and pharmaceutically acceptable salts thereof, are selective ligands for GABA A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
US20050196374 Defecation deodorant An orally ingestible defecation deodarant reduces the production of intestinal gas and the production of malodors accompanying defecation or the emanation of intestinal gas, by absorbing malodor causing substances from the gastrointestinal tract; prevents the occurence of constipation; and adsorbs substances from the gastrointestinal tract that interfere with the absorption of orally administered drugs, pharmaceuticals, and other active ingredients from the gastrointestinal tract into the bloodstream and/or body. The defecation deodorant contains at least one adsorbent selected from a chelate compound, coconut vinegar, food fiber, gelatin, polyphenol, and a plant extract, on the surface of activated carbon.
CN103408530A Coumarin skeleton polycyclic compound with biological activity as well as preparation method and use thereof The invention relates to a coumarin skeleton polycyclic compound with biological activity as well as a preparation method and use thereof. The general formula structure of the compound is as shown in the specification, wherein in the formula, * represents a chiral carbon atom, R1 and R2 are respectively any one of C1-C16 alkyl, heteroaromatic ring or substituted aromatic ring; R3 is any one of H or C1-C16 alkyl or aryl; R4-R7 are respectively any one of H, F, Cl, Br, ester group, cyano, sulfuryl, nitro, heteroaromatic ring, C1-C16 oxyl, C1-C16 alkyl or substituted aromatic ring, and X is any one of O, X N, S atoms or imine, ketoxime and aromatic hydrazone. The compound has excellent region and stereoselectivity and a plurality of special physiological activities and tumor cell proliferation inhibition activities, and can be used for researching and developing antitumor drugs.
US20050031667 biocompatible nonerodible polymeric device which releases dopamine agonist continuously with generally linear release kinetics for extended periods of time; Parkinson's disease; erectile dysfunction and restless leg syndrome The present invention provides compositions, methods, and kits for treatment of Parkinson's disease and other conditions for which treatment with a dopamine agonist is therapeutically beneficial. The invention provides a biocompatible nonerodible polymeric device which releases dopamine agonist continuously with generally linear release kinetics for extended periods of time. Dopamine agonist is released through pores that open to the surface of the polymeric matrix in which it is encapsulated. The device may be administered subcutaneously to an individual in need of continuous treatment with dopamine agonist.
CN103694367A Extraction and application methods of meretrix meretrix linnaeus polysaccharides with antioxidant activity The invention discloses a method for separating and purifying meretrix meretrix linnaeus polysaccharides, relating to the field of biological separation and purification technologies. The method mainly comprises the steps of carrying out added-enzyme assisted hot water extraction, suspended steaming concentration and ethanol precipitation on meretrix meretrix linnaeus soft-bodied homogenate, so as to obtain a crude meretrix meretrix linnaeus polysaccharide product, then, carrying out deproteinization by a sevage method, and gradually separating and purifying the meretrix meretrix linnaeus polysaccharides by adopting DEAE-52 cellulose anion-exchange column chromatography and Superdex 200 gel-filtration column chromatography, wherein the meretrix meretrix linnaeus polysaccharides obtained through purifying are single polysaccharides of two kinds and have the purity over 90%. Thus, the obtained refined meretrix meretrix linnaeus polysaccharide product can serve as raw materials or additives of pharmaceuticals, chemicals, healthcare nutrients and cosmetics; a basis is provided for further researching the meretrix meretrix linnaeus polysaccharides.
US20110269700 Glucoside derivatives and uses thereof The present invention relates to compounds of formula I and pharmaceutically acceptable salts thereof, and to formulations and uses of the compounds of formula (I) in the treatment of metabolic disorders.
CN102040517A Resveratrol derivative and application thereof to medicament The invention relates to a resveratrol derivative and application thereof to a medicament, and particularly discloses a compound shown as a formula I or pharmaceutically acceptable salt, ester, solvate and stereoisomers thereof. In the formula I, R1, R2 and R3 are independently selected from a hydrogen atom, C1 to C3 alkyl or a substituted group shown as a formula i; at least one of R1, R2 and R3 is the substituted group shown as the formula i; R is selected from the hydrogen atom, substituted or unsubstituted C1 to C5 alkyl, substituted or unsubstituted C3 to C6 naphthenic base, benzyl or phenyl; R4 and R5 are independently selected from the hydrogen atom, the substituted or unsubstituted C1 to C5 alkyl, or substituted or the unsubstituted C3 to C6 naphthenic base; and n is an integer of between 1 and 5. The invention also discloses a medicinal composition containing the compound shown as the formula I, and the application of the compound shown as the formula I to the preparation of a medicament for treating and/or preventing cardiovascular and cerebrovascular diseases. The compound shown as the formula I can be effectively used for treating and/or preventing the cardiovascular and cerebrovascular diseases such as hyperlipemia.
US20100012132 Clear, washable lubricant compositions, and methods of making same Bi- or multiphasic, clear or translucent silicone-containing lubricant compositions, condom products including such compositions and methods of making such compositions and condom products are disclosed. The refractive index of each immiscible phase of the lubricant composition is matched to that of each other phase to make the composition clear or translucent. The compositions are highly lubricious, non-staining, and easily washable.
US20110021490 Chromene compounds, a process for their preparationand pharmaceutical compositions containing them The invention relates to compounds of formula (I): wherein R1 and R2 together form the following carbon-containing chain: wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl, aryl, heteroaryl, 3,4-dioxocyclobutenyl, alkylcarbonyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, benzoyl, arylsulphonyl or heteroarylsulphonyl group, each of those groups optionally being substituted, or R3 and R4 together with the nitrogen atom carrying them form a 5- to 8-membered ring, the ring thereby formed optionally being substituted. Medicinal products containing the same which are useful in treating conditions requiring a D3 receptor antagonist.
EP1937366B1 Synergistic mixtures of bisabolol and ginger extract Described is a formulation having a skin irritation-reducing action consisting of or comprising: bisabolol and a composition or compound chosen from the group consisting of a) substance mixtures obtainable from an extraction of ginger, b) substance mixtures obtainable from a separation of a ginger extract which comprise a compound which is chosen from the group consisting of gingerols, shogaols, gingerdiols, dehydrogingerdiones, paradols and derivatives thereof and c) compounds obtainable from a separation of a ginger extract which are chosen from the group consisting of gingerols, shogaols, gingerdiols, dehydrogingerdiones, paradols and derivatives thereof and mixtures thereof, wherein the particular content of bisabolol and of the said composition or compound in the formulation is adjusted such that the skin irritation-reducing action of these contents is increased synergistically.
US20100310555 Compositions with hematopoietic and immune activity The present invention provides methods of using Bv8 and EG-VEGF polypeptides and nucleic acids to promote hematopoiesis. Also provided herein are methods of screening for modulators of Bv8 and EG-VEGF activity. Furthermore, methods of treatment using Bv8 and EG-VEGF polypeptides or Bv8 and EG-VEGF antagonists are provided.
US20120283293 Methods of neuroprotection involving Prostaglandin E2 EP4 (PGE2 EP4) receptor activation The present invention provides methods for attenuating neuronal inflammation and neuronal damage in case of acute or chronic injury of nerve cells of the central nervous system through prostaglandin E2 EP4 receptor activation. Methods for treating neuropathic pain are also provided.
WO2008046357A1 Aqueous solution containing sodium pyruvate, preparation method and use thereof A stable aqueous solution of sodium pyruvate for medical use, which contains 20-1200mM sodium pyruvate and a stabilizer of sodium pyruvate, wherein the said stabilizer is H+ which leads to pH3.5-6.0 or NaCl which provides at least 20mM Na+.
US20110171159 Glycoside Derivatives and Uses Thereof This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.
CN102516298A Stable pharmaceutical salt of L-aonitrate phosphate ester, its preparation method and application The invention relates to a stable pharmaceutical salt of L-aonitrate phosphate ester, its preparation method and application. The related strong acid salt of the L-aonitrate phosphate ester is shown by the formula I and is mainly used in treating anaerobic infection or protozoan infection.
US7166744 Retinoid derivatives and methods for producing said compounds and anti-cancer pharmaceutical composition comprising said compounds The present invention relates to a novel retinoid derivative compound represented by the formula I: wherein X, R1, R2 and R3 are as defined herein or pharmaceutically acceptalbe salts thereof. Also, the present invention relates to processes for producing the compound of the formula I and to an anti-cancer composition comprising the compound of the formula I. The compound of the formula I according to the present invention exerts high anti-cancer effects while not causing undesirable side effects.
CN1748707A Use of ivermectin in treating seborrhea and using method The ivermectin preparations for treating seborrhea include liniment and cream. The ivermectin liniment is water solution of ivermectin in the concentration of 750mcg/ml; and the ivermectin cream includes ivermectin in effective treating amount and supplementary material.
WO2010032448A1 Sheet for repairing cartilage defect site Provided is a method for producing a cartilage cell not undergoing hypertrophic differentiation and a cartilage cell sheet not undergoing hypertrophic differentiation which are to be used for repairing a damaged cartilage site due to, for example, arthrosis deformans. Also provided are a cartilage cell sheet which can promote cartilage regeneration and a method for producing the same. Also provided is an agent which promotes cartilage regeneration. It is found out that dedifferentiated cartilage cells can be redifferentiated by administering a compound represented as a thienoindazole derivative (hereinafter abbreviated as TM) to the dedifferentiated cartilage cells or undifferentiated mesenchymal cells. Also, it is found out that TM induces the initial differentiation of a cartilage and does not promote the hypertrophic differentiation of cartilage cells. Moreover, it is found out that TM enhances the expression of type 2 collagen that is a cartilage differentiation marker.
CA2749856A1 Isoxazole-3-carboxamide derivatives The present invention relates to isoxa-zole-3-carboxamide derivative having the general Formula I or a pharmaceutically acceptable salt there-of, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carbox-amide derivatives for the treatment of TRPV1 mediat-ed disorders, such as acute and chronic pain disor-ders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.
CN101292942A Dermatologic preparation composition containing gamma-oryzanol The purpose of the invention is to provide a skin external use agent compound which comprises gamma-oryzanol in oil phase and inhibits discoloration with time. The invention provides the skin external use agent compound comprising the gamma-oryzanol and sodium bisulfate.
CN102008454A Daidzein-entrapped PLGA nanoparticles and preparation method thereof The invention relates to daidzein-entrapped polylactic polyglycolic acid (PLGA) nanoparticles and a preparation method thereof in the technical field of nanomedicines. The nanoparticles comprise the following components in percentage by mass: 0.1 to 45 percent of daidzein, 25 to 95 percent of polylactic polyglycolic acid and 1 to 65 percent of pharmaceutic adjuvant, wherein the molecular weight of the PLGA is between 8,000 and 15,000, the polylactic polyglycolic acid is long-chain macromolecules in which the ratio of the lactic acid to glycollic acid is 50:50, and the pharmaceutic adjuvant is lecithin, cyclodextrin or polyvinyl alcohol (PVA). The daidzein-entrapped PLGA nanoparticles have the particle size of between 280 and 330 nanometers and concentrated particle size distribution, redissolved freeze-dried powder is not adhered, and the medicine loading rate of the PLGA nanoparticles is between 1 and 2 percent, and the encapsulating rate is between 80 and 84 percent.
CN102018709A Tablet capsules with Loratadine tablets and Ambroxol hydrochloride tablets The invention relates to oral hard capsules, in particular to tablet capsules filled with Loratadine tablets and Ambroxol hydrochloride tablets. Each tablet capsule consists of a capsule and a tablet in the capsule, wherein the capsule comprises an upper capsule body and a lower capsule body, and the capsule is at least filled with one tablet with the active ingredient of Loratadine and one tablet with the active ingredient of Ambroxol hydrochloride. The active ingredients in the capsule do not contact with one another, so chemical change and side products do not generate among all the active ingredients, the stability of the products is improved, and particularly, degradation products caused by the contact of the Loratadine and the Ambroxol are reduced; cylindrical tablets, different colors and a transparent capsule shell are adopted, so the products are very suitable for industrialized production and the compliance of patients is improved; and the tablets are prepared from the active ingredients respectively, so medicaments are detected easily and the quality is controlled easily.
CN1626092A Cefaclor oral desintegration tablet and preparation method Cefaclor An oral dinstegrating tablet of antibacterial cefacolor and its preparing process are disclosed.
US7709207 Method for identifying compounds for treatment of pain Methods and products for the attenuation or treatment of pain and the reduction of nociception are described. The methods and products are based on the modulation of CNS intracellular chloride levels. The methods and products may also relate to modulation of the activity and/or expression of a chloride transporter, such as the KCC2 potassium-chloride cotransporter. Also described herein are commercial packages and uses based on such modulation. Related methods for identifying or characterizing a compound for the treatment of pain, the reduction of nociception and the diagnosis and prognostication of pain are also described.
CN101513447A Medicament for treating dermatitis and tinea The invention discloses a medicament for treating dermatitis and tinea, which is a pharmaceutical composition prepared from pure natural plants, animals, mineral and chemical products. The medicament has the advantages of wide source and low cost of raw materials, and simple preparation method.
US20080039530 treating a mammal for a vascular permeability disorder by administering a vascular endothelial sphingosine-1-phosphate receptor agonist comprising 2-amino-2-[2-(4-octaphenyl)ethyl]propane-1,3 diol, or 2-amino-2-methyl-4-[4-heptoxy-phenyl]butane-1-ol Agonist of vascular endothelial sphingosine-1-phosphate receptors are described. Compounds such as FTY720 can be phosphorylated by sphingosine kinase-2 into the phosphorylated froms which serve as sphingosine-1-phosphate receptor agonists. The vascular endothelial sphingosine-1-phosphate receptor agonists are employed in methods of treating a mammal for vascular permeability disorders and unwanted vascular endothelial cell apoptosis, and for the growth of new blood vessels. The sphingosine-1-phosphate receptor agonists can be used for the manufacture of a medicament for treating vascular permeability disorders and unwanted vascular endothelial cell apoptosis, and for the growth of new blood vessels.
US7964609 Use of mGluR5 antagonists for the treatment of gerd The present invention relates to the use of metabotropic glutamate receptor 5 antagonists for the inhibition of transient lower esophageal sphincter relaxations. A further aspect of the invention is directed to the use of metabotropic glutamate receptor 5 antagonists for the treatment of gastroesophageal reflux disease, as well as for the treatment of regurgitation.
US20110064664 Methods and compositions involving chitosan nanoparticles Disclosed are nanoparticles for the delivery of a therapeutic agent or a diagnostic agent to a subject that include a chitosan and a polyphosphate, wherein the weight ratio of the chitosan to the polyphosphate is about 1.0 or greater and the weight ratio of the polyphosphate to the therapeutic agent or diagnostic agent is about 15.0 or less. Also disclosed are nanoparticles that include a chitosan and an inhibitor of enhancer of Zeste homologue 2 (EZH2). Methods of delivering a therapeutic agent or a diagnostic agent to a subject for the treatment or prevention of a disease and methods of predicting prognosis of ovarian cancer in a subject that involve determining the expression and/or function of EZH2 in the subject are also disclosed.
EP1274686B1 Process for preparing 2-(4-chlorobenzolamino) -3- 2(1h) -quinolinon-4-yl proprionic acid The invention relates to a novel method for preparing 2_(4_chlorobenzoylamino)_3_[2(1H)_quinolinon_4_yl] propionic acid, also known as Rebamipide represented by the formula I and useful for treatement of peptic ulcer from alkyl 2_(4_chlorobenzoylamino)_2_alkoxycarbonyl_3_[2(1H)_quinolinon_4_ yl] propionate represented by the formula II in the presence of a base solution for hydrolisis and decarboxylation to remove a carboxyl group:
CA2328314C Long chain alcohols admixed in sterol compounds The present invention provides a method of providing a desirable admixture of long chain alcohols and sterols in a food or beverage product. More specifically, this process comprises dissolving or suspending the long chain alcohol in the sterol, and then incorporating the admixture into food or beverage product.
US20110189201 Modulation of bone development Methods and compositions for modulating bone development are described.
US8012503 Administering propranolol or a derivative across a mucosal membrane in combination with a buffering agent (phosphate buffer) to provide a pH of 7.6 at the membrane; sublingual; cardiovascular disorders A method for enhancing absorption of a compound in a medicament that is suitable for administering transmucosally to a subject is conducted in an environment having a suitable pH. The suitable pH is determined based on the ionization constant (dissociation constant) of the compound in water, the solubility of the ionized form of the compound, and the solubility of the non-ionized form of the compound.
WO2007109844A1 Anti-inflammatory metal complexes There are described metal complexes of anti- inflammatory ligands useful in the treatment of one or more of inflammation, cancer, diabetes, cardiovascular and other conditions.
US7507725 Compounds with sulphonamide group and pharmaceutical compositions containing these compounds The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula —SO2NR1R2, wherein R1 and R2, independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high “first path” effect, to be administered orally effectively or significantly improve the oral activity thereof.
US8486937 Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and use thereof The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
EP1987811A1 Skin-whitening cosmetic Disclosed are: a novel skin-whitening agent; and a skin-whitening cosmetic or quasi-drug which is highly effective for prevention/amelioration of melanopathy and is prepared using the skin-whitening agent. The cosmetic contains a compound represented by the general formula (I) and /or a salt thereof as an active ingredient. In the general formula (I), R1 and R2 independently represent a secondary or tertiary alkyl group having 3 to 7 carbon atoms; and R3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms.
CN102070425A Diphenyl ketene and derivatives thereof serving as tyrosinase inhibitors and application thereof The invention discloses diphenyl ketene and derivatives thereof serving as tyrosinase inhibitors and application thereof. The chemical structures of the diphenyl ketene and the derivatives thereof are shown as formulas (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI), (XII) and (XIII) (XIV). The diphenyl ketene and the derivatives thereof have good inhibiting effect on tyrosinase serving as a key enzyme for catalyzing the synthesis of melanin organisms, good effects of whitening skin and dispelling freckles and low toxic or side effect; the preparation method is simple, and the raw materials are easily obtained; and the diphenyl ketene and the derivatives thereof are applied in whitening cosmetics, whitening and freckle dispelling medicaments and fresh keeping and browning prevention of food.
EP2481407A1 Compounds for use in treating cognitive disorders The present invention provides a compound represented by the following Formula 1 or a pharmaceutically-acceptable salt thereof for use in treating a cognitive disorder: wherein the symbols in Formula 1 have the definitions recited in Claim 1.
CA2259621C Isocoumarin derivatives and their use in medicines Compounds represented by general formula (I) and medicinal compositions thereof, wherein R represents hydrogen or C1-6 alkyl, and n is an integer of 0 or 1. These medicinal compositions are usable in the prevention or treatment of diseases accompanying immunonomodulatory abnormalities or neovascularization.
WO2013106349A1 Use of the aminoalkylindole jwh-073-m4 and related compounds as neutral cb1 recptor antagonists for the treatment of alcoholism, drug abuse, obesity, and obesity-related diseases Novel alkylindoles that bind tightly to cannabinoid receptors and are neutral antagonists for the cannabinoid 1 receptor and agonists for the cannabinoid 2 receptor are provided. These compounds are useful for treating alcoholism and drug abuse and for treating obesity.
EP2198879A1 CD74 modulator agent for regulating dendritic cell migration and device for studying the motility capacity of a cell The present invention relates to a method for regulating the dendritic cell motility and/or migration in vivo using a CD74 modulator agent. It also concerns a device for determining or studying the motility capacity of a cell and the use thereof. The CD74 modulator agent is of use in the treatment of auto-immune diseases, cancers, inflammatory diseases or viral infections.
US7641925 Mixture of Trigonelline, amino acid and soluble fibers A synergistic composition for the treatment of diabetes in a subject in need thereof, comprising Trigonelline of concentration ranging between 20 to 30%, amino acids of concentration ranging between 20 to 60%, and soluble fiber of concentration ranging between 10 to 60%, optionally along with pharmaceutically acceptable additives, a process thereof and also, a method of treating diabetes.
CN1772211A Cold fever eliminating injection The cold fever eliminating injection is prepared with giantreed rhizome, sweet wormwood, banbooleaf bupleurum root, gypsum, polysobate-80 and water for injection in certain weight proportion. Its preparation process includes the following steps: distilling sweet wormwood and banbooleaf bupleurum root and collecting distilled liquid; extracting giantreed rhizome and gypsum first with water and then with alcohol and concentrating to obtain concentrate; adding water for injection and active carbon to the concentrate, boiling and suction filtering to obtain clear filtrate; mixing polysobate-80 and distilled water, mixing with the filtrate, regulating pH value, and adding water for injection to required amount.
WO2011018495A1 New compounds for the treatment of cns disorders The invention relates to novel pyrazolopyrimidinones according to formula (I). The new compounds shall be used for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments for the treatment of Alzheimer's disease. Further aspects of the present invention refer to a process for the manufacture of the compounds and their use for producing medicaments.
CN101069676A Method for preparing brufen soft capsule The present invention discloses a preparation method of liquid soft capsule containing ibuprofen. Said ibuprofen soft capsule has high bioavailability, its absorption is rapid, its action is quick and its contents matrix is stable. Said method is characterized by that in the solvent an alkaline substance is added, and the produced hydroxide radical can make partial ibuprofen be ionized and existed in the solution in the form of salt and free so as to raise solubility of ibuprofen and greatly reduce irritation of ibuprofen to gastrointestinal tract.
EP2016081A1 Anti-viral pyrimidine nucleoside derivatives A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH2, Y is O, S or NH, Z is O, S or CH2, R1 is C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of R2 and R3 is OH, and the other of R3 and R2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R2 or R3 may be (IV): in which R4, R5, R6 and R7 are each independently H or C 1-2 alkyl. In preferred embodiments, one of R2 or R3 is valine, leucine, isoleucine or alanine, particularly valine.
WO2013173720A1 Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors The present invention provides piperidinylcyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I, as defined herein, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
US20060148732 Inhibition of NF-kappaB by triterpene compositions The invention provides methods for the inhibition of inflammation by providing, to a cell, in need thereof, monoterpene compositions that inhibit NF-κB. These compositions may also contain a carrier moiety that renders the monoterpene composition membrane permeable. The carrier may include triterpenoid moieties, sugars, lipids, or even additional monoterpenoid moieties. The composition can also contain additional chemical functionalities. Methods for using these compounds to prevent and treat a wide range of inflammatory conditions, especially, premalignant inflammatory conditions are described.
US7189408 phosphate functionalized (per)fluoropolyethers, capable to confer improved protective hydro/oil-repellence properties to the formulation itself Base compositions (premix) comprising the following components: A) a perfluoropolyether phosphate; B) a solvent; C) water.
US20090215736 inhibitors of apoptosis and IL-1 beta secretion; mediate cell apoptosis and inflammation; good cell penetration and pharmacokinetic properties; [3S/R(2S)]3-[2-(Carbazol-9-yl-2-oxo-ethyl)-pentanoylamino]-5-fluoro-4-oxo-pentanoic acid This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
US20110263712 Process for the preparation of vorinostat The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient vorinostat. In particular it relates to a process for preparing vorinostat substantially free from impurities, involving suberic acid, aniline and hydroxylamine as starting materials.
CN101945865A 1, 2, 4 -oxadiazole compounds for the treatment of autoimmune diseases The present invention relates to novel oxadiazole derivatives of formula (I) or a pharmaceutically acceptable salt thereof thereof. Compounds of formula (I) and their pharmaceutically acceptable salts are of use in the treatment of conditions or disorders which are mediated via the S1 P1 receptor. In particular the compounds of formula (I) and their pharmaceutically acceptable salts are of use in the treatment of multiple sclerosis, autoimmune diseases, chronic inflammatory disorders, asthma, inflammatory neuropathies, arthritis, transplantation, Crohn's disease, ulcerative colitis, lupus erythematosis, psoriasis, ischemia-reperfusion injury, solid tumours, and tumour metastasis, diseases associated with angiogenesis, vascular diseases, pain conditions, acute viral diseases, inflammatory bowel conditions, insulin and non-insulin dependant diabetes.
EP2473041A1 Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors In its many embodiments, the present invention provides a novel class of pyrimidine analogs as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention also includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the cell cycle checkpoint modulator as well as combinations and pharmaceutical kits. An example cell cycle checkpoint modulator is shown below: formula (I).
WO2007119656A1 Tamsulosin-containing percutaneous absorption type preparation A tamsulosin-containing percutaneous absorption type preparation. A percutaneous absorption type preparation comprising a support and an adhesive layer on the support, characterized in that the adhesive layer contains an acrylic adhesive, further contains tamsulosin as an active ingredient in an amount of 0.1 to 20% by mass of the total mass of the adhesive layer and, if desired, a polyoxyethylene alkyl ether which is an additive playing a role in increasing solubility and a propylene glycol fatty acid ester which is an additive playing a role in promoting percutaneous absorption is provided. Further, a percutaneous absorption type preparation comprising a support and an adhesive layer on the support, characterized in that the adhesive layer contains a synthetic rubber adhesive, further contains tamsulosin as an active ingredient in an amount of 0.1 to 20% by mass of the total mass of the adhesive layer and a propylene glycol fatty acid ester which is an additive playing a role in promoting percutaneous absorption is provided.
WO2010148963A1 Compounds having activity against hepatitis virus and use thereof Compounds represented by formula (I) or pharmaceutically acceptable salts or hydrates thereof, and use of the compounds in the manufacture of medicaments against virus, preferably hepatitis virus, such as hepatitis C virus and hepatitis B virus.
US20090298850 Treatment for Neurological and Mental Disorders Methods for treating neurological or mental disorders in humans and the symptoms associated therewith are provided by administering eltoprazine and/or related compounds. In some embodiments, specific symptoms are treated by administering eltoprazine and/or a related compound in an effective amount to ameliorate the symptoms. Of particular significance are symptoms that are associated with cognitive dysfunction where eltoprazine will improve the symptoms and the disorder associated with that symptom. Of particular interest are non-ADHD-associated inattention, hyperactivity and impulsiveness. The methods provided herein are especially useful for improving functional recovery after CNS injury such as stroke where improved cognitive function will facilitate the acquisition of learning and memory of rehabilitative tasks.
CN1843489A Vaginal capsule suppository for female The invention relates to a capsule for treating women's vaginal diseases, as well as the preparing process, wherein the capsule comprises contents and hard shells, the contents include oil of aromatic turmeric, borneo camphor and auxiliary materials.
US6986740 administering an ultrasound contrast agent such as Rose Bengal; a portion of the contrast agent being retained in tissue of interest; and imaging the tissue with ultrasound to identify the tissue New contrast agents for ultrasound imaging and methods for use of such agents for imaging of human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene or halogenated xanthene derivative. Preferably, the halogenated xanthene is Rose Bengal or a functional derivative of Rose Bengal.
CN102488684A Application of sumatriptan in preparation of medicines for preventing and treating narcomania The invention provides a novel application of sumatriptan or its pharmaceutically acceptable salt in preparation of medicines for preventing and treating opioid dependence symptoms. The invention also provides a novel application of a preparation containing sumatriptan or its pharmaceutically acceptable salt in preparation of medicines for preventing and treating opioid dependence symptoms. Compared with the current medicines for preventing and treating opioid dependence symptoms, the sumatriptan has the advantages of definite therapeutic effect as well as small toxic and side effect, and canbe an ideal drug rehabilitation medicine for administration.
WO2013165575A1 Fluorinated 2-amino-4-(benzylamino)phenylcarbamate derivatives The invention relates to fluorinated compounds and their use as anti-epileptic, muscle- relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.
CN1907281A Method for preparing lansoprazole intestine dissolving capsule The invention relates to a process for preparing lansoprazole enteric-coated capsules, which comprising mixing 0-100 micron lansoprazole raw material 20-30g, microcrystalline cellulose 80-150g, disodium hydrogen phosphate 1-5g, anhydrous sodium sulfite 1-5g, sodium dodecylsulfate 1-5g, L-arginine 3-12g to make active pellet cores, dressing lansoprazole onto the pellet cores, finally separating the dressing layer and the enteric-coating layer.
CN101601645A Method for preparing ceftiofur hydrochloride parenteral solution The invention relates to a method for preparing ceftiofur hydrochloride parenteral solution; the hydrochloride parenteral solution has the characteristics of even distribution and clear and transparent solution. The method comprises the following steps: (1) adding propylene glycol and ceftiofur hydrochloride with a volume equal to 60-70% of the total volume of ceftiofur hydrochloride parenteral solution to be prepared in a thick mixing tank; adding 2-10g ceftiofur hydrochloride for every 100ml of total volume of the ceftiofur hydrochloride parenteral solution; heating to 40-50 DEG C and stirring for rapid dissolving; (2) adding propylene glycol to reach the total volume of the ceftiofur hydrochloride parenteral solution to be prepared and cooling to 20-30 DEG C; (3) adding active carbon, stirring for 15-20 minutes and filtering; and (4) filling and sealing, sterilizing, light check and packing. The invention solves the problems of difficult and uneven injection of the ceftiofur hydrochloride parenteral solution of the existing technology and makes up the defects of easy-layer and inconvenient use of the ceftiofur hydrochloride suspension injection of the existing technology.
CN101953789A Dry suspension containing cefprozil liposome and preparation method thereof The invention relates to a cefprozil liposome, a preparation method thereof and a dry suspension containing the cefprozil liposome. The cefprozil liposome comprises cefprozil, hydrogenated soya bean lecithin, hydrogenated yolk lecithin, cholesterol and vitamin E in the weight ratio of 1:(1.25-5):(1.25-5):(2.5-10):(0.1-3). The dry suspension containing the cefprozil liposome not only conforms to the requirements of Chinese pharmacopoeia, but also has the advantages of more stable storage at normal temperature, rapider effect taking and obviously increased bioavailability compared with common cefprozil medicine compositions.
WO2012138713A3 Multifunctional radical quenchers for the treatment of mitochondrial dysfunction The present disclosure provides methods for identifying therapeutic agents that are multifunctional radical quenchers. It also provides compounds of formula (I), (II), or (II-A): and pharmaceutically acceptable salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
CN101407500A 3,4-diaryl isoxazole-5-amido derivative, and preparation and use thereof The invention provides 3, 4-diaryl isoxazole-5-amino derivatives. Natural product CA-4 is used as the lead compound, and 5-amino isoxazole ring replaces an ethylene coupling chain in the structure of CA-4 and is taken as a conformation restricted group, thus synthesizing a series of 3, 4-diaryl isoxazole-5-amino derivatives. Pharmacological experiments show that the derivatives have good in-vitro inhibition proliferation effect for various tumor cell strains, and a plurality of compounds have the function of inducing apoptosis and the application in preparing anti-tumor drugs. The 3, 4-diaryl isoxazole-5-amino derivatives have reasonable design and simple preparation, and are suitable for practical use. The structural general formula of the derivatives is shown in the right formula.
WO2014089450A1 Specific inhibitors of cdk3 The invention provides new compounds and methods for inhibiting Cyclin-Dependent Kinase 3 (CDK3), and new methods for identifying such compounds.
US20090047363 Deodorant Antibacterial Fibrous Product A deodorant antimicrobial fibrous product containing a cancrinite-like mineral containing an antimicrobial metal, a clay mineral, softwood bleached kraft pulp, and hardwood bleached kraft pulp. The weight ratio of the softwood bleached kraft pulp to hardwood bleached kraft pulp is preferably 95/5 to 50/50. The clay mineral is preferably zeolite, sepiolite or bentonite. The deodorant antimicrobial fibrous product is preferably in the form of a sheet or a broken piece thereof, a granule or a three-dimensional molding.
CN103540655A Application of MK5 gene for screening anti-liver cancer drug The invention belongs to the field of a biological medicine and relates to application of a human gene MK5 for screening and preparing a drug for inhibiting growth of liver cancer cell. The liver cancer is one of common tumors around the world at present. The quantity of patients who die of the liver cancer every year ranks the third place of the quantity of the patients who die of tumors. The MK5 disclosed by the invention has an effect of promoting a liver cancer cell to resist adriamycin-induced apoptosis, and can developed as a novel drug target for inhibiting growth of the liver cancer cell. SiRNA of the MK5 has an effect of promoting adriamycin-induced apoptosis of liver cancer cell, can be used together with adriamycin to inhibit growth and multiplication of the liver cancer cell or can be combined with the adriamycin to be used as a drug for promoting apoptosis of the liver cancer cell. The MK5 disclosed by the invention and an antagonist thereof can be used for preparing the drug for inhibiting growth of the liver cancer cell; a novel way and means are provided for treatment and detection of the liver cancer.
US20080045572 Pharmaceutical Composition Comprising Roflumilast or the N-Oxide of Roflumilast An aqueous pharmaceutical preparation for administration of a slightly soluble PDE4 inhibitor is described.
US6878387 Core with an organic acid salt; acrylic blend coating of an interpolymer of a (meth)acrylate ester and a quaternary ammonium (meth)acrylate and a (meth)acrylate ester homo- or copolymer with an ester having acid or base groups The invention relates to a pharmaceutical preparation consisting of: (a) a core containing an active substance, optionally an excipient and common pharmaceutical additives in addition to the salt of an inorganic acid whose proportion in the weight of the core ranges from 2.5 to 97% by weight and (b) and outer film coating consisting of one or more (meth)acrylate copolymers and optionally common pharmaceutical adjuvants, wherein 40 to 100% by weight of the (meth)acrylate copolymers consist of 93 to 98% by weight of radically polymerized C1- to C4-alkylesters of acrylic or methacrylic acid and 7 to 2% by weight of (meth)acrylate monomers with a quaternary ammonium group in the alkyl radical and that may be optionally present in a mixture consisting of 1 to 60% by weight of one or more additional (meth)acrylate copolymers different from the above-mentioned (meth)acrylate copolymers, consisting of 85 to 100% by weight of a radically polymerized C1- to C4-alkylesters of acrylic orethacrylic acid and optionally and optionally up to 15% by weight of additional (meth)acrylate monomers with basic groups or acid groups in the alkyl radical.
WO2006117609A3 Phenoxypropylpiperidines and -pyrrolidines and their use as histamine h3 -receptor ligands The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
WO2007100066A1 17β HSD type 5 INHIBITOR It is intended to provide a novel and excellent method of treating and/or preventing prostate cancer, prostate enlargement, acne, seborrhea, hypertrichosis, calvities, alopecia, sexual precocity, adrenal hypertrophy, multilocular ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and so on based on an effect of selectively inhibiting 17β HSD type 5. It is found out that an N-sulfonylindole derivative, in which a carbon atom in the indole group is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group, has a potent activity of selectively inhibiting 17β HSD type 5 and is usable as a remedy and/or a preventive for diseases, in which 17β HSD type 5 participates, such as prostate enlargement and prostate cancer without showing any side effect caused by a decrease in testosterone.
CA2597395C Method and composition for treating mammalian diseases and injuries caused by the over-expression of peroxynitrite The present invention provides a method for treating wounds and diseases in mammals, caused by mammalian cells involved in an inflammatory response, by altering indigenous in vivo levels of peroxynitrous acid, and salts thereof. The method comprises contacting the mammalian cells with a therapeutically effective amount of a reactive oxygen species mediator, wherein the reactive oxygen species mediator is selected from the group consisting of pyruvates, pyruvate precursors, a- keto acids having four or more carbon atoms, precursors of ce-keto acids having four or more carbon atoms, and the salts thereof, wherein mediation of reactive oxygen species results in mediation of peroxynitrous acid. The present invention further provides a pharmaceutical composition for treating wounds and diseases in mammals, caused by mammalian cells involved in an inflammatory response, by altering indigenous in vivo levels of peroxynitrous acid, and salts thereof.
CN1827617A Antivirus use of 17-(tetrahydrofuryl-2'-yl) methyl amine-17-demethoxy geldanamycin The invention relates to an antivirus action of 17-(tetrahydrofuran-2'-substituent) methylamine-17-demethoxygeldanamycin. The research result of antiviral activity displays that the said compound possesses strong antiviral activity and wide antiviral range, which establishes solid foundation for us to additionally research and develop the said compound as clinical effective antiviral drug in the future.
US20050222264 Anti-rhinovirus active agents Glyoxal derivatives for use in the prevention and treatment of Rhinovirus infections are herein disclosed.
WO2008144263A1 Potent indole-3-carbinol-derived antitumor agents Compounds and methods for treating cancer and inducing apoptosis in unwanted rapidly proliferating cells. The compounds are shown in formula (I): wherein X is hydroxyl or amino; Y is carboxyl or sulfonyl; R1, R2, R3, and R4 can be the same or different and are selected from hydrogen, halogen, methoxy, trifluoromethyl, hydroxyl and combinations thereof; R5, R6, and R7 may be the same or different and are selected from hydrogen, chloro, bromo, nitro, phenyl, amino, methoxy, and combinations thereof; and derivatives or metabolites thereof.
WO2006080323A1 Six-membered heterocyclic compound and the use thereof A compound that can be used as a pharmaceutical active ingredient effective in prevention and/or treatment of osteoporosis, a bone disease such as fracture, and further, glaucoma or ulcerative colitis, and is represented by the general formula (I): [Chemical formula 1] (I) [wherein T represents an oxygen atom or the like; V represents CH2 or the like; R01 to R04 represent a hydrogen atom or the like; A represents a linear alkylene group or a linear alkenylene group having 2 to 8 carbon atoms or the like; D represents a carboxyl group or the like; X represents an ethylene group, a trimethylene group or the like; E represents a -CH(OH)- group or the like; and W represents a -U1-(RW1)(RW2)-U2-U3 group (wherein U1 represents a single bond or an alkylene group having 1 to 4 carbon atoms or the like; RW1 and RW2 represent a hydrogen atom or the like; U2 represents a single bond, an alkylene group having 1 to 4 carbon atoms or the like; and U3 represents an alkyl group having 1 to 8 carbon atoms or the like) or a residue of a carbocyclic or heterocyclic compound]; or a salt thereof.
US20100183573 membrane polypeptide for use in designing therapeutic for proliferative, inflammatory, skin, arthritic, cardiovascular and autoimmune disorders; cancer, immunological-related, blood-related and skin-related disorders Novel polypeptides that are splice variants of c-Met, the receptor for hepatocyte growth factor and polynucleotides encoding same are provided. Methods and pharmaceutical compositions which can be used to treat various disorders such as cancer, immunological-related, blood-related and skin-related disorders using the polypeptides and polynucleotides of the present invention, are also provided.
EP1908481A1 Agent for reduction of bleeding in cerebrovascular disorder The present invention relates to a hemorrhage reducing agent in cerebrovascular disorder containing a poly (ADP- ribose) polymerase inhibitor (PARP inhibitor). The PARP inhibitor provides an inhibitory effect of vascular endothelial cell disorder so that it may reduce hemorrhage in cerebrovascular disorder. In addition, the PARP inhibitor inhibits the hemorrhage that is concerned about in thrombolytic agent use by using together with a thrombolytic agent, and an effect of extending therapeutic time window of a thrombolytic agent may be further expected. Furthermore, the PARP inhibitor can be a safe hemorrhage reducing agent with fewer side effects because it does not affect the blood coagulation system and the fibrinolytic system.
EP2233156A2 Use of aprotinin polypeptides as carriers in pharmaceutical conjugates Conjugates comprising carriers selected from the group consisting of aprotinin, a biologically active aprotinin fragment, Angiopep-1, Angiopep-2 and biologically active analogs, derivatives or fragments thereof and a label or drug are disclosed. Said conjugates increase the potency of the drug and modify the pharmacokinetics of the drug or label. The use of these conjugates in the treatment and diagnosis of cancer is described
WO2009014910A3 N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the rup3 or gpr119 receptor for the treatment of diabetes and metabolic disorders Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
EP2007352B1 Treatment of psychiatric patients with sleep disturbances and/or excessive daytime sleepiness with paliperidone The present invention provides a method for the treatment of psychiatric patients with excessive daytime sleepiness and/or a sleep disturbance comprising administering a therapeutically effective amount of paliperidone, its pharmaceutically acceptable acid addition salts, enantiomeric forms and esters thereof in a dosage form that provides a relatively low plasma concentration variation of paliperidone to the psychiatric patients in need of treatment.
CN1690066B Antiviral agent cidofovir derivatives The invention discloses a new derivant for antiviral cidofovir, as well as the method for making such derivant, which is taking key intermediate (S)-N1-[(3-trity methoxy-2-ethphosphoric acid methoxy)glycerol alcohol]-cytosine as raw material, to condensation react with Boc-amino acid with the help of condensating agent to get intermediate compound, and then stripping protecting group Boc and trityl, and hydrolyzing phosphate, after deacidizing it, reacting with chlorpivalmethylactone to get new derivant.
US20100008995 Processes for preparing pharmaceutical compositions A process for the production of a composition comprising a water-insoluble triptan which comprises the steps of: a) providing a mixture comprising: i) a water-insoluble triptan, ii) a water soluble carrier, and iii) a solvent for each of the triptan and the carrier, and b) spray-drying the mixture to remove the or each solvent and obtain a substantially solvent-free nano-dispersion of the triptan in the carrier.
CN101390866A Supplies for removing odor The present invention provides a recruit capable of being dissolved rapidly in stomach and reinforcing odor-eliminating effect by means of making the high chlorophyll quantity contained in one particle. The recruit is composed of a hard gelatin capsule (1) and a high-quantity phytol-removing chlorophyll (chlorophyll) powder (2) filled in the hard gelatin capsule. The hard gelatin capsule is edible hard gelatin capsule composed of gelatin, water and mold release (soya bean lecithin).
WO2014074976A1 Compositions and methods for treating neurological diseases or injury Provided are compounds for the treatment of neurological diseases or injuries, including neurodegenerative diseases, stroke, trauma, epilepsy, acute and chronic kidney injuries, diabetes mellitus, and/or seizures. In some embodiments, derivatives of vitamin K are provided.
US20100016253 Methods and compositions related to heightened apobec-1 related protein (arp) expression Disclosed are methods and compositions related to determining the status and mechanisms underlying long-term nonprogression of viral infections.
EP2782576A1 Sodium salt of (r)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1h-imidazol-4-yl)-propionic acid The invention relates to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid, and to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid which is in a crystalline form or in at least partially crystalline form, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor).
CN101890059A Hepatitis B virus resistant active composition of polyprenols from ginkgo biloba leaves and preparation method thereof The invention provides a hepatitis B virus resistant active composition of polyprenols from ginkgo biloba leaves and a preparation method thereof. The method is characterized by taking the liposoluble ginkgo biloba leaves with polyprenol content being lower than 40% as the raw materials, adopting activated carbon and attapulgite clay with mass ratio of 1:(1-20) as a mixed decoloring agent, carrying out decoloring for 10-80min at 50-120 while stirring, carrying out medium-pressure column chromatographic separation on the decolored polyprenols until the purity of the polyprenols is over 90% and taking ginkgo biloba flavonoids and terpene lactones as the auxiliary materials to prepare the active composition. The active composition has the effect of resisting hepatitis B virus and can be used for developing hepatitis B virus resistant drugs.
CN102940610A Vitamin B6 composition freeze-drying orally disintegrating tablets and preparation method thereof The invention provides vitamin B6 composition freeze-drying orally disintegrating tablets and a preparation method thereof, relating to the technical field of medicines and preparation method of medicines, mainly solving the problem that vitamin B6 preparations have bad curative effect, are not suitable for children and patients who have difficulty in swallowing in the prior art. The vitamin B6 composition freeze-drying orally disintegrating tablets comprise 0.5-5wt% of vitamin B6, 30-70wt% of mannitol, 2-4wt% of gelatin, 0.1-0.2wt% of sucralose, and 36-67wt% of purified water. According to the invention, the preparation process is simple, the components are simple, the prepared orally disintegrating tablets are suitable for children and patients who have difficulty in swallowing, and have the advantages of fast disintegration, fast effect, full medicine absorption, convenient administration, good mouthfeel, and first pass effect avoidance to the liver.
CN102846878A Preparation technology and production method for an integrated new formulation of angelica peony wine The invention relates to a preparation technology and production method for an integrated new formulation of angelica peony wine. The raw material composition of the active ingredients comprises (by weight parts) angelica 9, peony 30, tuckahoe 12, Rhizoma Atractylodis Macrocephalae 12, Rhizoma Alismatis 15, and chuanxiong 9. Its production process includes performing supersonic gas stream crushing, alcohol and water extracting, supersonic wave crushing and extracting, decoction concentrating, supersonic spray drying, nano-grinding, high-pressure homogenization, and nanoparticles preparation. The preparation technology and production method focuses on the multi-collaborative, multi-targeted advantages of nano-carrier coupling technique, can significantly reduce production costs, significantly improve the quality of products, make drug targeting property and slow controlled release property stronger after scale production, realize inside and outside administration, and can prepare into pellicle to paste on human blood to be directly absorbed through the skin.
CN103655525A Oral disinfectant The invention discloses oral disinfectant. The oral disinfectant consists of the following components in parts by weight: 2-5 parts of octane, 1-3 parts of decane, 5-10 parts of ethanol, 12-20 parts of sorbitol and 100-150 parts of de-ionized water. The oral disinfectant disclosed by the invention is low in preparation cost and good in disinfecting effect, and is applicable to preliminary disinfection of the oral cavity in a dental diagnosis and treatment process.
EP1071425B1 Treatment of depression and pharmaceutical preparations therefor It has been found that the treatment of depression using known SRIs and NRIs may be improved by the administration therewith of folic acid or a precursor which produces folate in the patient. The daily dose of NRI or SRI is as prescribed for treatment of depression in the usual way. The daily dose of the folic acid precursor should be such as to provide a folate dosage of 300-5000 micrograms/day.
US20080287542 Novel Isovaleramide Forms, Compositions Thereof, and Related Methods of Use The invention provides novel isovaleramide forms. These forms include isovaleramide co-crystals, and solvates, hydrates, co-crystals, and polymorphs thereof. The invention also provides novel compositions comprising these novel forms and one or more suitable carriers. The invention also provides related methods of treatment or prevention. Compositions and methods of the invention have a number of uses, including the treatment or prevention of epilepsy and anxiety.
US7776846 Administering a synergistic mixture of a cortisone, hydrocortisone and/or prednisolone derivative; antiasthmatic agents; side effect reduction Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17α-alkoxy-11β-hydroxyandrost-4-en-3-one-17β-carboxylate type and the corresponding Δ1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or β-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.
US20080194558 Quinazoline analogs as receptor Tyrosine Kinase inhibitors This invention concerns quinazoline analogs of Formula I: where an A group is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to three independent R3 groups. The invention also includes methods of using these compounds as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
CN103193647A Cancer pain treatment medicine with high optical purity The invention belongs to the technical field of medicine, and particularly relates to application of a high-optical-purity compound shown in a general formula (I) in preparation of a medicine for treating a cancer pain. R is defined in the specification. The invention also relates to a pharmaceutical composition including the compound.
WO2006078006A1 Indole compound and pharmaceutical composition containing the same As a compound excelling in oral absorption and having a β3- adrenaline receptor stimulating potency, there are provided compounds, or pharmaceutically acceptable salts thereof, of the formula: (I) wherein R1 is absent, or one or two or more thereof, identical with or different from each other, are present and represent a halogen atom, etc.; R2 is a hydrogen atom, etc.; each of R3, R4, R5 and R6 independently is a halogen atom, etc.; R7 is absent, or one or two or more thereof, identical with or different from each other, are present and represent a halogen atom, etc.; R8 is a hydrogen atom, or substituted or unsubstituted alkyl; and R9 is a substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc.
CA2750796A1 5-ht4 inhibitors for treating airway diseases, in particular asthma The invention relates generally to the treatment of diseases of the respiratory system such as asthma and chronic obstructive pulmonary disease. More particularly, the present invention relates to methods of treating and preventing asthmatic airway inflammation. The treatment involves the administration of a 5-HT4 receptor antagonist to the subject in need thereof; more in particular the administration of aroylated 4-aminomethylpiperidine derivatives as defined herein. Other aspects of the invention are directed to compositions for treating or preventing respiratory disorders, including pharmaceutical compositions.
EP1864979A1 Imidazole-derivatives as TAFAIa-inhibitors Imidazolyl-acetic acid derivatives (I) are new. Imidazolylacetic acid derivatives of formula (I) and their stereoisomers, mixtures and/or salts are new. U = H, 1-6C alkyl, 3-6C cycloalkyl, F, OCF 3 or CF 3; X = (A 1) m-A 2; Y = CH[6-14C aryl] 2, A 3-(A 4) o-(A 5) p, lactam of formula (a), CR 16R 17(CR 18R 19) x-C(O)NR 12R 13 or CR 26R 27(CR 28R 29) x-SO 2NR 24R 25; Z = H, 1-6C alkyl, 1-6C hydroxyalkyl, 3-6C cycloalkyl(0-4C alkyl), (1-10C alkylene)-OC(O)OR 1 or (CH 2) n-(6-14C aryl) or (CH 2) n-Het (both optionally substituted by 1-3 R 1); A 1 = (CH 2) n or O(CH 2) n; m = 0 or 1; n = 1-3; x = 0-3; y = 1-5; A 2 = 4-15 membered heterocyclic ring containing at least one N and substituted by amino, (optionally further substituted by 1-3 1-3C alkyl, halo, CF 3 or OCF 3), 1-6C aminoalkyl or 3-8C aminocycloalkyl; either (a) A 3 = 3-8C cycloalkyl or 2-6C alkynylene (optionally substituted (os) by 1-3 OR 10 or R 1), A4 = N(R 2) 2, A 5 is absent and o = 0 or 1; or (b) A 3 = 3-8C cycloalkyl (os by 1-3 OR 10 or R 1), A 4 = NR 2, A 5 = C(O)R 3, C(O)NR 4R 5, SO 2R 6 or C(O)OR 7, o and p =1; (c) A 3 = 3-8 membered cyclic amine (os by 1-3 R 1), A 4 and A 5 are as in (b) with A 5 bonded to the N atom of A 3, o = 0 and p = 0 or 1; (d) A 3 = (CH 2) q(6-14C aryl) optionally ring-substituted by 1-3 R 1, A 4 and A 5 are as in (b), o = 0 or 1, p = 1 and q = 1-3; (e) A 3 = (CH 2) r-Het1, A 4 and A 5 are as in (b), o = 0 or 1, p = 1 and r = 1-3; or (f) A 3 = (CH 2) q(6-14C aryl) optionally ring-substituted by 1-3 R 1, A 4 = O, A 5 = 6-14C aryl (os by 1-3 R 1), o, p = 1 and q =1-3; Het1 = 4-15 membered heterocycle os by 1-3 oxo or R 1; R 1 = 6-14C aryl (os by 1-3 1-6C alkyl, 3-8C cycloalkyl(0-4C alkyl), CF 3, O, OCF 3 or halo), 4-15 membered heterocycle, 1-6C alkyl, 3-8C cycloalkyl(0-4C)alkyl, CF 3, OCF 3 or halo; R 2 = 6-14C aryl, 1-6C alkyl or 3-8C cycloalkyl (all os by 1-3 R 1), CF 3 or H; R 3, R 6-R 8 = 1-6C alkyl, 6-14C aryl, 4-15 membered heterocycle or 3-8C cycloalkyl (all os by 1-3 R 1) or H; R 4, R 5 = 1-6C alkyl, 2-10C alkenyl, 6-14C aryl, 4-15 membered heterocycle or 3-8C cycloalkyl (all os by 1-3 R 1) or H; or R 4+R 5 complete a 3-8 membered ring optionally including 1 or 2 additional O, S or N; R 12 = 1-6C alkyl or Q-(0-3C alkyl) (all os by 1-3 R 1) and R 13 = 6-14C aryl(0-3C alkyl) or Het(0-3C alkyl) (both os by 1-3 R 1); or R 12 = H, 1-6C alkyl, 0-3C alkyl(6-14C aryl) or 0-3C alkyl(Het) (all os by 1-3 R1) and R 13 = CHR 8R 9; Q = 3-6C cycloalkyl, 6-14C aryl or heterocycle; R 8, R 9 = 6-14C aryl or heterocycle (both os by 1-3 1-4C alkoxy or R 1); R 16-R 19 = H, 1-6C alkyl (os by 1 or 2 R 1), halo, OH, amino, 0-3C alkyl(6-14C aryl) or 0-3C alkyl-Het (all os by 1-3 R 1); or R 16+R 17 or R 18+R 19 = 3-6 membered ring; R 24, R 25 = H, 1-6C alkyl (os by 1-2 R 1), 0-3C alkyl(6-14C aryl or Het), os by 1-3 R 1, or 0-3C alkyl(3-6C cycloalkyl); or R 24+R 25 complete a 3-8 membered ring that may contain 1 or 2 additional O, S or N; R 26-R 29 = H, 1-6C alkyl (os by 1 or 2 R 1), halo, OH, amino, or (0-3C alkyl)-6-14C aryl or -Het (all os by 1-3 R 1); or R 26+R 27 or R 28+R 29 = 3-6 membered ring. An independent claim is also included for preparation of (I). [Image] [Image] - ACTIVITY : Thrombolytic; Anticoagulant; Cardiant; Antianginal; Cerebroprotective; Antiarteriosclerotic; Antidiabetic; Cytostatic; Ophthalmological; Vulnerary. - MECHANISM OF ACTION : TAFIa inhibitor (activated thrombin-activatable fibrinolysis inhibitor). 3-(6-Aminopyridin-3-yl)-2-(1-cyclohexyl-1H-imidazol-1-yl)propionic acid, when tested using Actichrome Plasma TAFI Activity kit, had IC 50 against TAFIa of 0.03 mu M.
US7973031 Leukemia therapy ;myelodyspastic syndrome The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.
CN101444485B Gemcitabine liposome and preparation method thereof The invention relates to gemcitabine liposome and preparation method thereof, aiming at resolving problem of low entrapment rate of the existed gemcitabine liposome. The constitute of gemcitabine liposome comprises gemcitabine, phospholipid and cholesterin. Blank liposome is made by phospholipid and cholesterin. The weight ratio of gemcitabine and phospholipid is 1:(2-80), 1:(40-80) after being optimized. The gemcitabine liposome is made by ammonium sulphate gradient method.
US20120276195 Indole Alkaloid Derivatives Having Opioid Receptor Agonistic Effect, And Therapeutic Compositions And Methods Relating To Same Indole alkaloid derivatives having an opioid receptor agonistic effect, their synthesis, and therapeutic compositions containing these derivatives, and methods of treating conditions with these compounds and therapeutic compositions, are provided.
CN1857217A Slow released anticancer injection containing estrogen receptor antagonist The slow released anticancer injection containing estrogen receptor antagonist consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent contains suspending agent. The effective anticancer component is estrogen receptor antagonist selected from Fullvesrant, Eximestane, etc or the composition of estrogen receptor antagonist and estrogen receptor antagonist synergist selected from taxane, alkylating agent and/or plant alkaloid. The slow releasing supplementary material is selected from difatty acid-sebacic acid copolymer, EVAc, polylactic acid, etc. The suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for lowering systemic toxic reaction, raising local concentration optionally and rising chemotherapeutic and/or radiotherapeutic effect.
EP1471871B1 Treatment of neurological dysfunction comprising fructopyranose sulfamates and erythropoietin Co-therapy for the treatment of neurological dysfunctions comprising administration of one or more fructopyranose sulfamates and erythropoietin.
WO2013049096A1 Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds.
US20090124626 Pharmaceutical agent comprising insulin resistance improving agent To provide a method for treating diabetes which has an excellent hypoglycemic action and causes minimal adverse drug reactions, there is provided a medicine comprising a DPP-IV inhibitor and an insulin sensitizer in combination.
US20090215627 Crystal Structure of Biotin Carboxylase (Bc) Domain of Acetyl-Coenzyme a Carboxylase and Methods of Use Thereof A crystal comprising a biotin carboxylase domain of acetyl-CoA carboxylase is described, along with a computer-based method for identifying compounds that modulates activity of acetyl-CoA carboxylase, a computer-based method for rationally designing a compound that modulates activity of acetyl-CoA carboxylase, along with compounds produced by such methods, as well as compositions and methods of use thereof.
CN1771924A New Western medicine prepn for treating type-II diabetes The present invention relates to medicine compositions containing metformin as active component and one or several pharmaceutically acceptable excipients. These medicine compositions are suitable for treating non-insulin dependent diabetes.
CN1631367A Freeze dried powder injecta of doxofylline and its preparation The invention relates to a freeze dried powder injection of doxofylline and its preparation, wherein the injection comprises Doxofylline 0.05-0.5g, and at least one pharmaceutically acceptable excipient, pH modifier, anti-oxidant agent, and stabilizer, and is provided in the form of unit amount in the container. The advantages of the invention include easy medicament transport and preservation, prevention of freezing of the liquid injection in winter, increased medicament stability, thus can be applied for effectively treating bronchial asthma, lungs disease of bronchospasm, and chronic clogged pulmonary diseases.
CN103509005A Quinazoline compound as well as preparation method and application thereof The invention relates to the technical field of medicines, particularly to a quinazoline tyrosine kinase inhibitor, a preparation method of the quinazoline tyrosine kinase inhibitor and application of the quinazoline tyrosine kinase inhibitor in preparation of antitumor drugs. The compound has a structural formula (I) as shown in the specification. The compound disclosed by the invention has an excellent tyrosine kinase inhibiting activity, and particularly has the inhibiting activities on VEGFR1, VEGFR2 and VEGFR3, the absorption characteristic research in a Caco-2 model and the research on the metabolic rate of liver microsome are also conducted on part of the preferential compound.
EP0946170B1 Diclofenac for the treatment of vasculopathies The present invention is directed to preventing the nonenzymatic glycation of albumin, which generates biologically active Amadori glucose adducts in the albumin molecule, as well as methods of using compounds that protect albumin against nonenzymatic glycation to prevent vasculopathy. The present invention also is directed to preventing the nonenzymatic glycation of apolipoprotein B in low density lipoproteins, which generates Amadori glucose adducts in the apo B molecule that predispose to lipid oxidation and to LDL-cholesterol internalization leading to foam cells, as well as methods of using compounds that protect apo B/LDL against nonenzymatic glycation to prevent atherosclerosis and to reduce serum cholesterol levels.
CN101190916B Anticancer compound, preparation method and use thereof, and composition containing the compound The invention provides compounds of the same class with anticancer activity and purposes thereof. In particular, the invention solves the current defects of temozolomide and can significantly prolong the lives of patients with brain cancer and strengthen the treatment responses of the patients to the temozolomide. The invention combines the effect of inducing apoptosis of tumor cells of NO based on the anti-tumor effect of the temozolomide and applies the basic theories of drug design so as to design and synthesize NO-donating temozolomide nitrate esters derivatives with novel structure and NO releasing activity, namely the synthesis and anti-tumor activity of 3,4-dihydro-3-Methyl-4-oxoimidazo (5,1-d) 1,2,3,5 tetrazine-8-carboxylic carbonate.
US20110293556 Treatment of insulin resistance/metabolic syndrome to alleviate the risks of dementia This invention relates to Applicant's discovery that Metabolic Syndrome , a cluster of disorders stemming from a resistance to insulin, contributes directly to dementia, particularly Alzheimer's disease. Applicant's invention includes a screening method to determine susceptibility and diagnosis of dementia based on the risk factors for Metabolic Syndrome. Applicant's invention further includes methods for the prevention or treatment of dementia and other neurological conditions based on (1) minimizing insulin resistance, thereby preventing excess biosynthesis of insulin; (2) modulating the activity of IDE such that insulin competes less efficiently with β-amyloid protein for the TDE; and (3) blocking the consequences of NMDA receptor activation, such as by minimizing the generation of NO and other harmful free radicals.
US20090202566 Use of the ENDO-180 gene and polypeptide for diagnosis and treatment This application is directed to a process of identifying a compound capable of modulating activity of a human ENDO180 receptor that comprises the steps of measuring the binding of the ENDO180 receptor to an interactor with which the ENDO180 receptor interacts specifically in vivo, in the absence or presence of a compound, and determining whether the binding of the ENDO180 receptor to the interactor is affected by the compound. This application is also directed to use of a compound identified by that process in the preparation of a medicament for therapy of disease, in particular fibrosis. This application also relates to the use of ENDO180 modulators in treatment of disease.
US20120027785 Chimera comprising bacterial cytotoxin and methods of using the same This invention provides, a recombinant polypeptide encoding a chimera. The chimera includes a DNase I fragment or a homologue thereof and a Cdt fragment or a homologue thereof. Further, the invention provides methods, utilizing the recombinant polypeptide encoding the chimera, such as a method for inhibiting the proliferation of a neoplastic cell, a method for treating a neoplastic disease in a human subject, a method for inhibiting or suppressing a neoplastic disease in a human subject, and a method for reducing the symptoms associated with a neoplastic disease in a human subject.
US7329760 CC-1065 analog synthesis Improved synthesis of seco(−)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2-dihydro-3H-benz(e)indole): and improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.
CN101270151B Peptide medicaments for accelerating medulla hematopoiesis cell proliferation The present invention provides a peptide drug that can promote the proliferation of marrow hematopoietic cells. The main amino acid sequence of the short peptide fragments, analogs, derivants and variants of the short peptide is larger than or equal to 70 percent, equal to and larger than or equal to 90 percent similar to the main amino acid sequence of the short peptide. The short peptide, nucleotides, short peptide fragments, short peptide analogs, short peptide derivants and short peptide variants are used for the preparation of drugs for treating manifold marrow hematopoietic cell defection diseases, congenital anaemia, aplastic anemia and various hemorrhagic anemia diseases and can be applied to the bone marrow transplantation of leukemia patients, etc., that is, the peptide drug of the present invention can treat pancytopenia caused by hemopoietic stem cell defects.
US8609694 Use of pyridin-2-yl-methylamine derivatives for the production of a medicament for the treatment of chronic pain symptoms of neuropathological or psychogenic origin This invention relates to a treatment of chronic pain symptoms, especially of neuropathological or psychogenic origin, with pyridin-2-yl methylamine derivatives or pharmaceutically acceptable additive salts thereof.
CN1771973A Composite medicine containing nonsteroidal anti-inflammatory analgetic and its prepn The present invention constitutes compound medicine with nonsteroidal anti-inflammatory analgetic with aminoglucose and nonsteroidal anti-inflammatory analgetic. Compared with aminoglucose or nonsteroidal anti-inflammatory analgetic, the compound medicine of aminoglucose and nonsteroidal anti-inflammatory analgetic has raised curative effect, lowered toxic side effect, and raised patient compliance. The prepared eye preparation may be also used for noninfectious inflammation of eyes.
CN101773494A New application of green tea polyphenol The invention provides new application of green tea polyphenol in preventing and treating psychological stress injuries, which further shows that the green tea polyphenol has application in preparing medicaments or foods for preventing and treating symptoms or diseases correlative with the psychological stress injuries. The green tea polyphenol can improve the prolongation of latency and the reduction of grill-passing times and erection times of a Wistar rat in an open field test in a psychological stress state; the latency is prolonged and the number of electric shocks is increased in a step-through test; and the performance that the time for finishing a water maze and the number of errors are obviously increased is abnormal, which shows that the green tea polyphenol can improve the space exploration capacity, the cognitive function and the learning and memory ability of a psychological stress animal, has the effect of preventing and treating the psychological stress injuries, and is hopeful to be used for preparing the medicaments or the foods for preventing and treating the symptoms or the diseases correlative with the psychological stress injuries.
EP1667697A2 Method to treat the side effects associated with non steroidal anti-inflammatory drugs using microorganisms of the genus bifidobacterium. The present invention relates to the use of a microorganism and/or a metabolite thereof to at least increase the amount of a COX-1 mRNA in a cell. The present invention further relates to the use of a microorganism and/or a metabolite thereof in the manufacture of a medicament to treat the side effects associated with nonsteroidal antiinflammatory drugs (NSAIDs). The present invention further relates to a pharmaceutical preparation comprising in combination a nonsteroidal antiinflammatory drug (NSAIDs) and a microorganism and/or a metabolite thereof which is capable of at least increasing the amount of a COX-1 mRNA in a cell. The present invention yet further relates to a pharmaceutical preparation comprising in combination betaine or a pharmaceutically acceptable salt thereof and a microorganism and/or a metabolite thereof which is capable of at least increasing the amount of a COX-1 mRNA in a cell. The microorganism may suitably be a bacterium, preferably from the genus Bifidobacterium.
EP1098642B1 Diamino-propanol-compounds for treating ischemia The present invention includes methods for treatment and prophylaxis of conditions associated with lactosylceramide. The methods generally provide for administration to a mammal, particularly a human, of a therapeutically effective amount of a compound that increases enzymatic activity of UDPGal:GlcCerβ1→4 galactosylceramide (Ga1T-2). In vitro and in vivo assays for detecting compounds with therapeutic capacity to modulate Ga1T-2 are also provided.
CN103027889A Container-holding mesylate pazufloxacin aqueous solution and preparation method thereof The present invention relates to a container-holding mesylate pazufloxacin aqueous solution. The mesylate pazufloxacin aqueous solution is stored in a container with a seal, and is characterized in that the pH of the aqueous solution is in the range of 1-4, the concentration of mesylate pazufloxacin in the aqueous solution is 0.001-0.01 g/ml, the container is sealed by complex membrane or a coating film rubber stopper, and the film used by the complex membrane or the coating film rubber stopper is fluoro-polymer film, poly-p-xylene-containing film or composite polyethylene glycol terephthalate film. The present invention solves the problem that visible foreign matter appears in the mesylate pazufloxacin injection products during placement.
WO2008078091A1 Bicyclic heterocyclic compounds as fgfr inhibitors The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
WO2012060594A3 Anti-inflammatory composition containing a thiourea compound and a pharmaceutically acceptable salt thereof as an active ingredient 【Abstract】 The present invention relates to a pharmaceutical composition for preventing or treating inflammatory diseases, wherein the pharmaceutical composition contains, as an active ingredient, a thiourea compound represented by the following Formula 1 or a pharmaceutically acceptable salt thereof. The thiourea compound or pharmaceutically acceptable salt thereof, according to the present invention, reduces the activity of NF-kB that causes inflammatory diseases in a fibroblast-type synoviocyte and a mouse model of collagen induced arthritis, and effectively inhibits edema and pain. Thus, the composition of the present invention can be usefully used in preventing and treating inflammatory diseases such as rheumatoid arthritis.
US20100203164 Therapeutic Treatment of Cancer and Dysplasia of the Cervix or Vagina Using Estrogen Antagonists A method for treatment of cervical or vaginal cancer and their associated dysplasia, including the steps of identifying a human cervical or vaginal cancer and/or dysplasia patient, administering an effective amount of an estrogen antagonist therapy to the patient, wherein the amount is effective to reduce cancer and dysplasia symptoms, and observing a reduction of cancer and dysplasia symptoms in the patient.
WO2007048326A1 Nanometer targeted drug for magneto-thermotherapy of malignant tumors A magnetic nanoparticle of targeted drug and its preparation method, in which effector molecules and orienting molecules are incorporated in a weight ration of 1:0.0001-0.20. The said effector molecules are magnetic powders with a particle diameter less than 1000nm and specific absorption rate (SAR) from 10 to 7000W/gFe, the said oriented molecules include antibodies, ligands and magnetic powders, and the particle size of the targeted drug is from 2 to 1000nm. The preparation method involves getting the oriented molecules coupled onto the magnetic powders in water or organic/inorganic solvent or mixtures thereof according to the above weight ratio. The resulting nanometer magnetic powders of targeted drug can be used in the mild and high temperature magneto-thermotherapy against tumors as a result of efficiently killing malignant cells.
US20060128608 Novel chemical compounds and their use The present invention relates to prodrugs of pharmaceutical moieties, more specifically antimicrobial agents, methods for their preparation, pharmaceutical formulations containing them and their use in the treatment of microbial infections.
US20130331354 Method and composition utilizing larch wood extracts in animal feed A method for improving animal feed efficiency, efficiency of animal digestion, overall health of animals, and animal feed production efficiency. The method includes administering an effective amount of a feed additive composition having a combination of a dietary fiber and a flavonoid to an animal. The animal feed composition includes a Larch Arabinogalactan in an amount between 0.1% and 30% of the animal feed composition, a Dihydroquercetin (taxifolin) in an amount between 0.1% and 10% of the animal feed composition, and an animal feed carrier or an excipient.
CA2598821C Organoselenium containing compounds and their use The present invention relates to an organoselenium compound represented by the formula I below, a preparation method thereof and a medical composition comprising the compound as active ingredient. The organoselenium compound of the present invention has activity for peroxisome proliferator activated receptor .delta. (PPAR.delta.). (SEE FORMULA I)
US20080287401 Methods for Synthesizing and Purifying Aminoalkyl Tetracycline Compounds Methods for the synthesis and purification of 9-amino alkyl tetracycline compounds are described.
US7479282 Polypeptide comprising the amino acid of an N-terminal choline binding protein a truncate, vaccine derived therefrom and uses thereof This invention provides an isolated polypeptide comprising an amino acid sequence of a N-terminal choline binding protein A truncate in which the amino acid sequence is set forth in any of SEQ ID NOS: 1, 3-7, or 9-11, including fragments, mutants, variants, analogs, or derivatives, thereof. Also, this invention provides a isolated polypeptide comprising an amino acid sequence of a N-terminal choline binding protein A truncate, wherein the amino acid is set forth in SEQ ID NO: 24, wherein the polypeptide retains its native tertiary structure and methods of preparation. This invention provides an isolated polypeptide comprising an amino acid sequence of a N-terminal choline binding protein A truncate, wherein the polypeptide has lectin activity and does not bind to choline. This invention provides an isolated immunogenic polypeptide comprising an amino acid sequence of a N-terminal choline binding protein A truncate. This invention provides an isolated nucleic acid encoding a polypeptide comprising an amino acid sequence of a N-terminal choline binding protein A truncate. Lastly, this invention provides pharmaceutical compositions, vaccines, and diagnostic and therapeutic methods of use.
US20130029921 Inhibiting peptides derived from trem-like transcript 1 (tlt-1) and uses thereof The present invention relates to polypeptides fragments derived from the protein TLT-1 and their uses for the treatment of inflammatory conditions and more particularly for the treatment of sepsis.
CN102860778A Food sterilization wet wipe suitable for hand-mouth contact The invention discloses a food sterilization wet wipe suitable for hand-mouth contact and relates to the field of daily living equipment. The problems that the conventional sterilization product and wet wipe irritate the skin surface and are unsuitable for cleaning food and oral cavity can be solved. The food sterilization wet wipe comprises a wet wipe solution and a wet wipe solution carrier, and is characterized in that the raw material for preparing the wet wipe solution comprises the following components in percentage by weight: 0.4 to 0.6 percent of xylitol, 0.8 to 1.2 percent of sodium chloride, 0.04 to 0.07 percent of coconut oil amphiprotic disodium hydrogen diacetate, 0.04 to 0.07 percent of sodium fluoride, 0.01 to 0.03 percent of essence, 0.08 to 0.2 percent of potassium sorbate and the balance of water. The non-woven fabric serves as a carrier, a food-grade fungicide potassium sorbate is used, the food sterilization wet wipe is safe and reliable to use, does not contain alcohol and is natural and non-irritative; according to the addition of the xylitol, the food sterilization wet wipe is fresh in taste; and moreover, normal saline is used, and the cellular water in the oral cavity is kept. The food sterilization wet wipe is suitable for wiping hands, lip, oral cavity and other human parts which are easily infected by germs and wiping things which can be contacted by the skin or mouth, can achieve a protection function effectively, and prevents the bacteria attack.
CN103110938A Autologous biomedical fibrin glue preparation for plugging digestive tract fistula as well as preparation method and application of autologous biomedical fibrin glue preparation The invention discloses autologous biomedical fibrin glue preparation for plugging digestive tract fistula as well as a preparation method and application of the autologous biomedical fibrin glue preparation. The autologous biomedical fibrin glue preparation comprises the following components: FG (Fibrinogen) component I-Fibrinogen, 1mg/ml tranexamic acid solution and FG component II-thrombin, wherein the fibrinogen and the thrombin are prepared from high-concentration platelet-rich plasma. The invention further discloses the application of the autologous biomedical fibrin glue preparation for plugging digestive tract fistula in preparing medicaments or medical apparatus and instruments for treating full-digestive tract fistula. The invention has the following advantages: the preparation method is simple and easy to apply, the preparation cost is low, and the needs of the mass are satisfied; the biomedical fibrin glue is taken from a patient, so that the blood transfusion risks of heterologous blood products or xenogenous blood products are avoided; and besides, the biocompatibility is better, and no report about the adverse reaction exists until now according to the clinical tests.
CN101502532A Application of triple spiral Dictyophora phalloidea polysaccharide The invention provides bamboo fungus triple-helix polysaccharide and application thereof to the medicinal aspects of anti-tumor treatment and immunity function improvement. The bamboo fungus triple-helix polysaccharide is derived from natural bamboo fungi, wherein, the molecular weight thereof is 300,000 to 1,000,000; the bamboo fungus triple-helix polysaccharide has an ordered triple-helix structure; the monosaccharide composition thereof is glucose; and the backbone chain thereof has a Beta-(1->3) connection structure, and the branched chain thereof has a Beta-(1->6) connection structure with the branching coefficient being 10% to 20%. The invention discovers and verifies the triple-helix structure of the bamboo fungus polysaccharide, furthermore, by analyzing the results from the in vitro experiments of tumor cells through resisting S-180 tumor cells, the bamboo fungus triple-helix polysaccharide has obvious effect of inhibiting the S-180 tumor cells, which is equivalent to the effect of lentinan, an existing medicament for common clinical use, therefore, the invention has wide application prospect in the aspects of medicine and material.
US20050075335 Pharmaceutical composition comprising n((1-n-butyl-4-piperidinyl)methyl)-3,4-dihydro-2h-(1,3)oxazino(3,2-a)indole-10-carboxamide or salt and process therefor comprising dry granulation The invention provides a process for preparing a pharmaceutical composition comprising N-[(1-nbutyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carbixamide (pharmaceutical composition) (piboserod) or a pharmaceutically acceptable salt thereof in combination with one or more pharmaceutically acceptable excipients, the process comprising forming part or all of the (pharmaceutical composition) or the salt thereof into granules by a dry granulation process. The process is preferably a roller compaction process, preferably followed by milling to a suitable particle size. The granules are usually of increased particle size and/or compacted compared to the SB 207266 or the salt thereof. Preferably, the (pharmaceutical composition) or the salt thereof is present in the composition and/or in the granules in at least 4 weight % and/or up to 60 weight % by weight of the composition and/or by weight of the granules respectively. An intragranular lubricant, filler (e.g. CaHPO4), and/or compression aid (e.g. microcrystalline cellulose) are usually used. The invention also provides a pharmaceutical composition obtainable by the dry granulation process and/or which has been prepared by the dry granulation process.
US20080161290 Serine hydrolase inhibitors Provided herein are benzoxazinone compounds of formula I and compositions containing the compounds. The compounds and compositions are useful in the methods of inhibiting the action of serine hydrolase, including neutrophil elastase. In certain embodiments, the compounds and compositions are useful in the prevention, amelioration or treatment of serine hydrolase-mediated diseases.
US20110189260 Use of zinc chelators to inhibit biofilm formation A method is provided for inhibiting formation of a biofilm of bacteria, the method including contacting the bacteria with an effective amount of at least one zinc chelator, wherein the bacteria contain at least one zinc adhesion module, whereby formation of the biofilm is inhibited. A method for inhibiting biofilm formation on a device and a topical pharmaceutical composition for the inhibition of biofilm formation are also provided.
WO2011101408A1 Method for preventing cancer metastasis The present invention relates to the use of a specific family of glycerolipid compounds of formula (I) described in the detailed description or the manufacture of a medicament for the prevention or for the treatment of cancer metastasis.
CN201426858Y Clopidogrel hydrogen shlfate and aspirin double-layer tablet The utility model relates to a double-layer tablet, which comprises an aspirin sustained-release tablet layer and a copidogrel hydrogen shlfate rapid-release tablet. The utility model has simple preparation process, is convenient for patients to take and has accurate dose.
US20050112187 Nucleic acid that expresses a polypeptide such as a cytokine and a phospholipid, both having cytotoxic activity; synergistic combination; side effect reduction The present invention relates to a combination product comprising at least one nucleic acid containing a sequence encoding a polypeptide or interest and at least one phospholipid of interest, for use which is simultaneous, consecutive or spread out over time, characterized in that said polypeptide and phospholipid of interest have cytotoxic activity.
US7563913 Compound and pharmaceutical composition There are provided novel compounds that have been extracted and isolated from a plant belonging to the family Compositae. Compounds represented by general formula (I): wherein R1 represents hydroxyl and R2 represents methoxy.
CN1748701A New method for producing pyritinol hydrochloride for injection The process of producing pyritinol hydrochloride for injection includes the following steps: dissolving pyritinol hydrochloride in recipe amount in injection water; ultrafiltering; adsorbing with active carbon; filtering with microporous filtering membrane; bacteria-free packing the filtrate in vial; and freeze drying. While bacteria-free filtering, the insoluble particles in the medicine liquid are also eliminated, and this can greatly reduce the phlebitis attacking probability. The product is loose and well water soluble.
US20080015159 Small Synthetic Rna, a Method of Preparing the Same and Uses Thereof Translation of the hepatitis C virus (HCV) RNA is mediated by the interaction of ribosomes and cellular proteins with an internal ribosome entry site (IRES) located within the 5′untranslated region (5′UTR). We have investigated whether small RNA molecules corresponding to the different stem-loop (SL) domains of the HCV IRES, when introduced in trans, can bind to the cellular proteins and antagonize their binding to the viral IRES, thereby inhibiting HCV IRES-mediated translation. We have found that an RNA molecule corresponding to SL III of the HCV IRES could efficiently inhibit HCV IRES-mediated translation in a dose-dependent manner without affecting cap-dependent translation. The SL III RNA was also found to bind efficiently to most of the cellular proteins which interacted with the HCV 5′UTR. A smaller RNA corresponding to SL e+f of domain III also strongly and selectively inhibited HCV IRES-mediated translation. This RNA molecule showed strong interaction with the ribosomal S5 protein and prevented the recruitment of the 40S ribosomal subunit by the HCV IRES. In conclusion our results demonstrate a novel approach to selectively block HCV RNA translation using a small RNA molecules mimicking the structure of the stem-loop IIIe+f subdomain of the HCV-IRES. The discovery provides a basis for developing a potent antiviral therapy targeting the interaction between the ribosome and the HCV-IRES RNA.
EP1858870A1 Semi-synthetic taxane derivatives with antitumor activity The invention discloses novel secotaxane derivatives of general formula 1, having cytotoxic activity, which can be administered through the injective or oral route, for the therapy of tumors.
CN1867564B Process for preparing amino crotonyl compounds The invention relates to an improved method for the production of 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-butene-1-yl]amino}-7-((S)-tetrahydrofurane-3-yloxy)-quinazoline and related amino crotonyl compounds. The invention also relates to a suitable salt of 4-[(3-chloro-4-fluorphenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-butene-1-yl]amino}-7-((S)-tetrahydrofurane-3-yloxy)-quinazoline for use as an active ingredient for a medicament.
WO2010132879A2 Multicomponent degradable cationic polymers Degradable polymers were synthesized that self-assemble with DNA to form particles that are effective for gene delivery. Small changes to polymer synthesis conditions, particle formulation conditions, and polymer structure provides significant changes to efficacy in a cell-type dependent manner. Polymers presented here are more effective than commercially available materials, such as LIPOFECTAMINE 2000™, FUGENE®, or polyethylenimine (PEI), for gene delivery to cancerous fibroblasts or human primary fibroblasts. The presently disclosed materials may be useful for cancer therapeutics and regenerative medicine.
US20090252694 Novel Chalcone Derivatives, Pharmaceutically Acceptable Salt, Method for Preparation and Uses Thereof Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of: reacting aminoacetophenone with sulfonylchloride under the presence of an appropriate salt; and reacting the compound prepared in the above step with hydroxybenzaldehide under the presence of an appropriate catalyst. The chalcone derivative of formula 1 in accordance with the present invention having strong enzyme inhibitory activities for glycosidase can be effectively used in preventing and treating various diseases induced by glycosidase, and the chalcone derivative of the invention having tyrosinase and melanin synthesis inhibitory activities can be effectively used as a skin-whitening compound.
CA2341031C Novel salt form of pantoprazole The invention relates to the dihydrate of the magnesium salt of pantoprazole. Pantoprazole has the following chemical structure:(See formula I) The novel compound (also referred to as pantoprazole magnesium dihydrate) is useful for the treatment and prevention of diseases which are considered to be treatable or avoidable by the use of pyridin-2-ylmethylsulfinyl-1H-benzimidazoles. In particular, the novel compound can be employed in the treatment of disorders of the stomach or the intestine.
US20100215724 Microcapsule Nanotube Devices for Targeted Delivery of Therapeutic Molecules A nanotube device comprises a gel matrix that includes microcapsules and functionalized nanotubes, or other functionalized nanostructures incorporated into said gel matrix. Pharmaceutical compositions and methods of treatment comprising same. The pharmaceutical compositions of the present invention enable the specific and targeted delivery of therapeutic agents such as DNA molecules, peptides, including antibodies, drug molecules (e.g. small organic molecules), while offering sufficient resistance towards mucus layer of the intestine and high concentrations of enzymes and other molecules found in the blood stream and the GI tract.
CN102462667A Clopidogrel bisulfate tablet The invention relates to a clopidogrel bisulfate tablet. A preparation method of the clopidogrel bisulfate tablet comprises the following steps of mixing clopidogrel bisulfate, lactose and hydroxy propyl cellulose according to a weight ratio of 1: (0.02 to 1): (1 to 3), preparing the mixture into pellets, dressing the pellets, and pressing the dressed pellets and an appropriate amount of magnesium stearate into tablets. Compared with the prior art, the preparation method adopts a pellet dressing and tabletting technology, improves product stability and curative effects, and prevents the sticking problem produced in drug tabletting.
CA2637083A1 Use of naphthyridine derivatives as medicaments Compounds of formula (I) in free or salt form for the preparation of a medicament for the treatment of pulmonary hypertension, where R1 and R2 have the meanings as indicated in the specification. Pharmaceutical compositions that contain the compounds are also described.
US20100129288 Gliomedin, Fragments Thereof and Methods of Using Same The present invention relates to pharmaceutical compositions comprising gliomedin and active fragments thereof, polynucleotides encoding gliomedin, host cells expressing gliomedin, antibodies to gliomedin and small interfering RNA (siRNA) molecules that down regulate the expression of gliomedin and methods of using same. The present invention also provides methods of treating and diagnosing neurological disorders using the pharmaceutical compositions and antibodies of the invention.
US20080107626 Adjuvant agent for hepatitis C An adjuvant agent is used in combination with interferon and ribavirin for treating hepatitis C. The adjuvant agent contains 50 to 90 wt % cordyceps sinensis, and also contains 10 to 50 wt % astragalus membranaceus. The cordyceps sinensis used to prepare the adjuvant agent is isolated from the culture of the asexual form of Hirsutella sinensis mycelium.
US20100234472 Nitric oxide releasing derivatives of paracetamol The present invention particularly relates to novel nitrate esters of paracetamol. The nitrate esters of paracetamol are prepared by reacting the paracetamol with dihaloalkyl compound and followed by reaction with silver nitrate to obtain the corresponding nitrate ester derivatives. The nitrate esters of paracetamol are useful as analgesic, anti-inflammatory agents.
WO2006046888A3 Preparation for curing stomatological diseases The invention relates to curing general stomatological diseases such as gingivitis, parodontitis and periodontosis without surgical interferences. The inventive medicinal preparation comprises 40-75 mass % zinc oxide, the rest being a vegetable oil. In the preferred embodiment, the vegetable oil is embodied in the form of a sea buckthorn oil. Said invention makes it possible to efficiently cure gingivitis, parodontitis and periodontosis associated with the osseous tissue regeneration. Said preparation is easily producible and usable.
US20080125496 Antimicrobial flavor and oral care composition containing the same The present invention provides antimicrobial flavors and flavor compositions which are of high safety and little influential on intestinal bacteria, as well as oral care compositions and foods containing the same. The flavor is selected from dihydrofarnesol, isocamphylcyclohexanol, levosandol, bacdanol, Santalinol, methyl atrarate, 10-undecen-1-ol, 2-methyl undecanal, sandalol, dodecanal, brahmanol, neroridol, o-methoxycinnamic aldehyde, methyl sandeflor, 9-decen-1-ol, 3-dodecenal, etc.
CN102861051A Application of Houttuynoid A in medicine for treating renal cancer The invention discloses application of Houttuynoid A in preparing a medicine for treating renal cancer, which belongs to the technical field of new application of the medicine. According to the assessment on the antineoplastic activity through in-vitro MTT method, Houttuynoid A has an obvious inhibiting effect on the growth of human renal cancer cell strain KC. Therefore, Houttuynoid A can be used for preparing the medicine for preventing renal cancer, and has a favorable development and application prospect. The application of Houttuynoid A in preparing the medicine for treating renal cancer, which is provided by the invention, is disclosed for the first time, and because the skeleton type belongs to brand-new skeleton type, the inhibiting activity of Houttuynoid A to renal cancer cells is extremely strong.
WO2014013903A1 Liquid composition containing taxane-based active ingredient, process for producing same, and liquid medicinal preparation A liquid composition which comprises (a) a taxane-based active ingredient selected from the group consisting of docetaxel and derivatives thereof, (b) at least one glycol, and (c) at least one surfactant ingredient selected from the group consisting of polysorbates, polyoxyethylene glycol esters, and polyoxyethylene castor oil derivatives, wherein the volume ratio of the glycol (b) to the surfactant ingredient (c) is in the range of 45/55 to 55/45 and the total content of the glycol (b) and the surfactant ingredient (c) is 95 v/v% or higher relative to the whole volume of the liquid composition.
EP2067779A1 Tiotropium salts, method for their production and medicinal formulas containing them Preparation of new tiotropilium salts (1) by subjecting a different tiotropilium salt (2) to anion exchange with an ion source in a solvent. Preparation of new tiotropilium salts of formula (1) by subjecting a different tiotropilium salt of formula (2) to anion exchange with an ion source (Kat-X) in a solvent. [Image] X : anion; Y : anion, different from X, i.e. halo, 1-10C alkyl-sulfonate or -sulfate, or 6-10C arylsulfonate; Kat : cation. An independent claim is also included for new compounds (1) and (2), except where Y/X = bromo, optionally as solvates or hydrates. - ACTIVITY : Antiasthmatic. No details of tests for antiasthmatic activity are given. - MECHANISM OF ACTION : Anticholinergic.
CN102198124A Gromwell extract for treating rheumatoid arthritis, and soft capsules thereof The invention discloses a gromwell extract and a preparation method thereof. The gromwell extract contains 0.10-25% of acetylalkannin, 0-20% of isovalerylalkannin, 0-20% of alpha-methylbutyrylalkannin and 0-30% of beta,beta-dimethylacrylalkannin (counted by a high performance liquid chromatography peak area normalization method). The invention also discloses soft capsules taking the gromwell extract as a raw material and a preparation method of the soft capsules. The invention also discloses an application of the gromwell extract in preparing a medicament for treating rheumatoid arthritis.
WO2008117773A1 Process for production of asymmetric tetrasubstituted quinolonecarboxylic acids and intermediates for the production The invention makes it possible to produce, industrially and easily, optically active compounds for constructing substituents in the production of extremely safe quinolone- carboxylic acids having high antibacterial activity. Intermediate compounds represented by the general formula (5) are produced by treating a compound represented by the general formula (3) in the presence of a metal catalyst and a hydrogen source (wherein n is 2 to 5; R1 is alkyl or aryl; R6 is alkyl, aryl, or hydrogen; and one of R71 and R72 is aryl and the other is aryl, alkyl, alkenyl, aralkyl, or hydrogen). (3)(5)
US20080064743 Dry powder compound formulations and uses thereof The present invention provides lyophilized formulations comprising methylnaltrexone, and processes for preparation of provided formulations. Additionally provided are compositions and products containing the methylnaltrexone formulation, as well as methods for producing formulations, compositions and products. Provided formulations as well as compositions and products containing methylnaltrexone formulations are useful for preventing, treating delaying, diminishing or reducing the severity and/or incidence of side effects resulting from administration of analgesic opioids.
US20130065865 Barrier film-forming germicidal composition for controlling mastitis A long-lasting persistent, uniform film-forming skin protecting germicidal composition provides a long-lasting persistent barrier film when applied to skin. The compositions have particular utility as barrier teat dips for protecting cows against mastitis. A barrier film-forming agent is selected from the modified or hydrolyzed polysaccharides, particularly a hydrolyzed or modified starch, such as dextrin and maltodextrin. The barrier film-forming agent is stably solubilized in a solvent that dries to form the long-lasting persistent uniform film over the animal skin. The compositions also contain antimicrobial agents that fight against microbes that manage to penetrate the protective barrier film. Particularly, advantageous is that all the materials used are safe food additive and cost effective over the traditional barrier film forming agents.
WO2009014217A1 Bicyclic pyrrole derivative Disclosed is a compound represented by the formula (I) below which is useful as a renin inhibitor, or a pharmaceutically acceptable salt thereof. In the formula (I), G represents a group represented by the formula (a') below or the like; R1a represents an optionally substituted C1-10 alkyl group or the like; R1b, R1c, R1d and R1e may be the same or different and independently represent a hydrogen atom or the like; R1f represents a hydrogen atom, a halogen atom or the like; R2 represents an optionally substituted C1-6 alkyl group or the like; R3a, R3b, R3c and R3d may be the same or different and independently represent a group -A-B (wherein A represents a single bond or the like and B represents a hydrogen atom, an optionally substituted C1-6 alkyl group or the like) or the like; and n represents 1 or the like.
CN101007164A Compound ofloxacin injection and its preparation method The invention disclosed a kind of complex ofloxacin injection as well as preparing method. The injection contains 5-20 shares of ofloxacin, 5-25 shares of sulphuric acid colistin, 1-20 shares of trimethoprim and 50-300 shares of propylene glycol. The preparing procedure includes the following steps: (1) weighing materials; (2) putting the sulphuric acid colistin into injection water, stirring until it's all soluble; (3) heating propylene glycol to 75-85DEG C, adding trimethoprim, stirring to make it soluble; (4) putting together the solution of step (2) and (3), clarifying the solution, regulating the ph value of the solution, adding water to 1000 shares to get the preparation. Ofloxacin has the antibacterial activity of the third generation quinolones which can inhibit the bacteria prokaryotic cell DNA gyrase and DNA replication. Sulphuric acid colistin has no residue and side effects in animal bodies. The combination of the two medicines can widen the antibacterial spectrum and increase the curative effect.
US20050064031 Combination contraceptive, kits that contain the latter, and a method that uses the latter This invention relates to a multi-phase combination preparation that contains at least 28 daily dosage units: with a first phase of at least 21 initial daily dosage units, containing a competitive progesterone antagonist in a dosage which inhibits ovulation during the first above-named phase; and a second phase of 5 to 28 daily dosage units, in which each dosage unit of this second phase contains a gestagen, as well as a corresponding package (contraceptive kit) that contains this combination preparation and a contraceptive method which uses the combination preparation above.
CN103070832A Cisatracurium besylate lyophilized preparation composition stable at room temperature and preparation method thereof The invention relates to a Cisatracurium besylate lyophilized preparation composition stable at room temperature and a preparation method thereof. The lyophilized preparation contains benzene sulfonic acid Cisatracurium besylate and a lyophilization excipient, a weight ratio of the lyophilization excipient to the benzene sulfonic acid Cisatracurium besylate (W / W) is 1:1-5:1. The lyophilized preparation overcomes the defect of cryopreservation of an existing lyophilized preparation, and is convenient for hospitals and patients for storage. The lyophilized preparation is used for muscle relaxation for operation patients.
US20110218164 Therapeutic, dietary or cosmetic use of compounds with specific anti-apoptotic activity toward caspase-3, and compositions containing these compounds This invention regards the use of zeaxanthin and/or rutin, as such or further combined with spermidine, as the active principle in a pharmaceutical, dietary, or cosmetic composition, acting to inhibit caspase-3 and therefore to control apoptosis by preventing programmed cell death. The indication for this composition according to the invention is primarily the treatment of scalp disorders characterized by excessive cellular turnover including chemotherapy-induced alopecia, alopecia areata, androgenetic alopecia and telogen effluvium.
US20100075925 Hyperthermic Technologies And Therapeutic Uses Thereof The present invention provides nanoscale and microscale compositions useful for a variety of purposes, including the diagnosis and treatment of diseases. In one embodiment, the present invention provides a disease treatment system comprising a thermal induction agent and a radiation source, wherein the thermal induction agent comprises at least one carbon nanotube, at least one carbon microtube, or a mixture thereof.
CN101361751B Moisture absorption self-adhesion barrier film capable of preventing postoperative adhesions and preparation method thereof The invention discloses an isolating film of hygroscopicity and self-adhesion which is used for preventing postoperative synechia. The isolating film is characterized by comprising 65 percent to 99 percent of carboxylation chitosan, 1 percent to 10 percent of glycerin, 0 percent to 5 percent of citric acid, and the rest being water. The preparing steps are as follows: weighing the ingredients by weight percentage; adding the carboxylation chitosan into water and stirring for thorough dissolution; adding the other ingredients into the solution and stirring; pouring the mixed solution into a glass mold for self-leveling, drying the solution for forming film and then cooling to room temperature; and at last, stripping the film from the mold. The isolating film is bacteria-free; when being implanted in human bodies, the film immediately absorbs tissue fluid once in contact with surface of wound, thus having viscidity. The isolating film which is simple and convenient in clinic can be automatically adhered on surface of wound which needs isolating. Therefore, the isolating film has the efficacy of promoting wound healing and preventing tissues from adhesion.
CN1640406A Drug-dropping and intelligence-promoting medicine using ocotillol as effective component, and its preparing method and use The present invention provides a medicine using ocotillol as effective copmonent for stopping drugs and raising intelligence. Said invention also provides its preparation method and its application.
WO2006025517A1 Sodium channel inhibitor A sodium channel inhibitor containing as an active ingredient a piperidine derivative or a pharmaceutically acceptable salt thereof. Also provided is the derivative or salt. The derivative or salt has a structure in which the piperidine ring is directly bonded to a benzene ring or heteroring and this benzene ring or heteroring is directly bonded to another benzene ring. The compounds not only have a high analgesic effect on neurogenic pains but are reduced in side effects.
CN101891785B Extraction method of hyperin and application thereof in medicament preparation The invention relates to an extraction method of hyperin and application thereof in medicament preparation. The extraction method of the hyperin comprises the following steps: placing Turpinia formosana leaves or Hypericum perforatum in 30%-90% ethanol of 5-15 times, carrying out reflux extraction for 1-3 times, and filtering, wherein the reflux extraction of each time is carried out for 1-3 hours; merging the filtrates, recovering the ethanol, eluting the aqueous solution with a macroporous adsorption resin column, collecting eluted parts, carrying out depressurized concentration, and drying to obtain mixed total glycoside of the hyperin; and carrying silicagel column chromatography and Sephadex LH-20 column chromatography separation, merging hyperin fractions, and crystallizing to obtain the pure hyperin product. The hyperin can be used as a neuraminidase inhibitor for preventing and treating flu, and can be prepared into pharmaceutically acceptable dosage forms.
CN102000342A Preparation method of superparamagnetism conductive nano gamma-ferric oxide/ polyaniline-dexamethasone sodium phosphate The invention discloses a preparation method of superparamagnetism conductive nano gamma-ferric oxide/ polyaniline-dexamethasone sodium phosphate, relating to the technical field of synthesis of superparamagnetism conductive nano gamma-ferric oxide/ polyaniline-dexamethasone sodium phosphate. The superparamagnetism conductive nano gamma-ferric oxide/ polyaniline-dexamethasone sodium phosphate is prepared by a doping method. The product of the invention can better suspend in water, still has favorable electrochemical activity and electric conduction magnetoconductivity within the pH range of human body environment, and can directionally reach diseased tissues under the regulation and control of an external magnetic field without damaging normal clasmatocyte. The targeted medicine is hopefully applied to treating acute leukemia, malignant lymphoma, connective tissue diseases, rheumatoid arthritis and the like. In addition, the method of the invention is simple, convenient, economical and favourable for industrial production and application.
US20130045214 P53 modulator and cancer target Methods of screening for modulators of TRIM24 (also known as TIF1-ALPHA) expression and/or biological activity are described. In particular, methods of screening for modulators of TRIM24 E3 ligase activity, and specifically an E3 ligase activity directed at p53 as the target polypeptide are also described. Modulators of TRIM24 expression and activity are provided and their use in treatment of cancer, particularly in breast, colon, prostate, renal cancers and in acute lymphoblastic leukemia. Suitable modulators of TRIM24 expression include siRNA and shRNA and can be used in the treatment of cancer and for targeting cancer stem cells.
WO2006095922A1 Tetrahydroisoquinoline compound and medicinal use thereof A tetrahydroisoquinoline compound, in particularly, a novel compound represented by the formula (I) (wherein the symbols are as defined in the description), or a pharmaceutically acceptable salt of the compound. They have excellent ACAT inhibitory activity and/or antioxidizing activity. (I)
WO2011081373A3 Method for preparing highly pure anhydrous crystalline docetaxel A method for preparing highly pure anhydrous crystalline docetaxel is provided. The method for preparing highly pure anhydrous crystalline docetaxel enables preparation of anhydrous crystalline docetaxel that has purity of 99.5% or more, and is useful as an anticancer agent due to remarkably low residual solvent content compared to the standard of residual solvents in drugs.
CN101940576A Compound and medicinal use thereof The invention relates to a compound and medicinal use thereof. The compound has a structural formula, is prepared by extracting Xuezhikang capsules and has HMG-CoA reductase inhibition activity.
EP2074994A1 Enhanced ocular neuroprotection/neurostimulation A macrolide-analogue with neuro-stimulatory and/or neuroprotective activity for use in partially or completely enhancing restoration of corneal sensation in the eye of a patient following laser assisted in situ keratomileusis (LASIK). The administration is non-systemic, localised ocular administration.
US20110177028 Interferon-beta and/or lambda for use in treating rhinovirus infection in the elderly Use of interferon-beta (IFN-β) and/or IFN-λ for treating rhinovirus (RV) infection in elderly people, particularly elderly people who are, or have been long-term smokers, especially those who have a clinical history of recurrent RV infections, and may have other medical conditions, such as cardiac or circulation problems, and who are liable to suffer severe complications/high mortality from poor innate ability to fight such a viral infection.
WO2010088574A1 Azabenzimidazoles and related analogs as sirtuin modulators Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin- modulating compound in combination with another therapeutic agent.
WO2011009020A3 Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.
US7049335 3-azabicyclo[3.1.0]hexane derivatives The subject invention provides a compound of the formula I, wherein X, Q, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined. Compounds of formula I have activity as opioid receptor antagonists. The subject invention furthermore provides for pharmaceutical compositions and therapeutic methods comprising compounds of formula I.
CN101390850B Hepatinica for tilapia Disclosed is a hepatinica for tilapia, which is characterized in that the hepatinica is composed of the followings by weight percentage: 35-45% betaine, 25-35% of taurine, 10-15% of L-carnitine, 8-12% of vitamin E and 6-10% of inositol. The hepatinica can protect the liver function obviously and promote the growth of tilapia and be used as feedstuff additive in tilapia feedstuff with the additionquantity of 0.1-0.3% so that the dosage of plant protein in feedstuff can be improved greatly; the feedstuff cost is reduced; the raw material has stable source and low price; the production process is simple.
CN101229133A Omeprazole sodium freeze-dried powder injection and preparing method thereof The invention provides an omeprazole sodium freeze-dried injection and a preparation method which is simple and feasible and the prepared freeze-dried injection is high in drug contents and low in related substances content. The method comprises the following steps: (1) the raw materials of the recipe quantity are stirred with injection water until the omeprazole sodium is completely dissolved to get omeprazole sodium solutions; sodium citrate solutions are put into the solutions got from step (1) and the pH value of the solutions is adjusted to 10.0 to 11.0; the injection water is put into the prepared products got from step (2) to the recipe quantity and then pin activated carbon is put into the prepared products, and filter decarburization is carried out after stirring to get filtrates; the filtrates got from step (3) are fine filling filtered by 0.22Mum removal bacteria microporous membrane, and the filtrates after fine filling filtering are put into a bottle which is partially stoppered, and then the filtrates are freeze-dried to get the freeze-dried injection.
CN103372010A Application of Chukrasone B in preparation of medicines for treating acute gout The invention provides a new application of Chukrasone B in medical science, and particularly relates to an application of the Chukrasone B in the preparation of medicines for treating acute gout. Experimental research results show that the Chukrasone B has a protection effect on the human vascular endothelial cell damaged acute grout caused by monosodium urate and can be used for inhibiting the expression of ICAM-1 (Intercellular Cell Adhesion Molecule-1), therefore, the Chukrasone B can be used for the preparation of the medicines for treating acute gout inflammation. The application of the Chukrasone B in the preparation of the medicines for treating the acute gout is disclosed by the invention for the first time. As the skeleton type of the Chukrasone B belongs to a bran-new skeleton type and the Chukrasone B has unexpected strong activity on the prevention and treatment of the rheumatoid rhinitis, the possibility that other compounds provide revelation does not exist. The Chukrasone B has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for preventing and treating the acute gout.
CN101397241A Ent-abieta diterpenoid largeleaf rabdosia leaf I and J, preparation method and use thereof The invention relates to corydalis and corydalis of isodon macrophylla which are extracted and separated from the isodon macrophylla and have the structural formula of ent-abietane diterpenoids, a preparation method and applications thereof. A plurality of in vitro anti-tumor activity experiments show that the compounds have significant effect of inhibiting the activity of tumor cells and can be applied in the preparation of medicaments for treating cancers and/or tumors. The invention can also provide the lead compounds for developing new medicaments for treating various common multiple cancers, thereby having important significance on developing and utilizing medicinal plant resources of China.
CN103006558A Cabazitaxel lipid microsphere injection and preparation method thereof The invention discloses a Cabazitaxel phospholipid complex and a method for preparing a lipid microsphere injection which contains the phospholipid complex. The lipid microsphere injection consists of Cabazitaxel, injection phospholipid, injection oil, an emulsifying agent, a stabilizing agent, an antioxidant, an isoosmotic adjusting agent and water for injection. The lipid microsphere injection has the characteristics of high drug-loading rate, slow releasing, small adverse reaction, simplicity and practicability in preparation technology, good product stability and the like and is beneficial to clinic application and industrial production.
CN101283987B Chloroquine liposomes freeze-dried powder injection and preparation method thereof The invention provides a chloroquine liposome lyophilized powder for injection, comprising (by weight parts) the chloroquine or the salt formed by the chloroquine and acid 1part, phospholipid 2-100 parts, cholesterol 1-35 parts, vitamin E 0.5-5.0 and excipients. The preparation method comprises two steps, including the preparation of blank liposome, and the preparation of drug-carrying liposome through the pH gradient method. The injection has the advantages of reasonable design, wide carrier selection range, high drug entrapment efficiency, and good stability. The preparation method has the advantages of easy operation, low cost, and good controllability and repeatability.
CN101234125A Method of preparing granulation physiotherapeutic salt The invention discloses a preparation method of a physiotherapy salt, which separates oval granule products with a particle size of 2.5-5mm from refined salts prepared with four stages vacuum evaporation technology through prepressing, mould pressing, crushing and shaping. Compared with the conventional refined salt, the granulation physiotherapy salt prepared via the method is characterized in large particle size and big density, thus having good moisture-resistance ability and anti-caking ability, and the granulation physiotherapy salt is of higher enthalpy, slow heat release and longer constant temperature time, which is more suitable for physiotherapy. At the same time, the method of the invention prepares the shape of the physiotherapy salt to be spherical granule, resulting in a structured shape, which is more favorable for improving the anti-caking ability and heat preservation ability, and more favorable for using in the mode of direct contact with human body.
WO2012035436A1 Plinabulin prodrug analogs and therapeutic uses thereof Compounds of Formula (I) and (I') are disclosed, as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed. (Formula (I) & (I'))
US20070286841 Method for lowering serum glucose A method for treating hyperglycemia and/or reducing serum glucose levels in a patient that includes administering to the patient a therapeutically effective amount of an amine polymer is disclosed. In one embodiment, the amine polymer is aliphatic. Examples of polymers useful in an embodiment of the invention include sevelamer hydrogen chloride and colesevelam. The invention includes the use of amine polymers such as a cross-linked polymer characterized by a repeat unit having the formula: and salts and copolymers thereof, where n is a positive integer and x is zero or an integer between 1 and about 4. Also described is a use, for the manufacture of a medicament, of a polymer that lowers serum glucose.
WO2008057291A2 Crystalline and amorphous imatinib base, imatinib mesylate- and processes for preparation thereof The present invention provides crystalline forms of imatinib base, imatinib base free of desmethyl imatinib, and imatinib mesylate free of desmethyl imatinib mesylate, processes of their preparation and pharmaceutical compositions of imatinib mesylate.
US20120064128 Nano-metallic alloy delivery system for treatment of infected cells and legions A system for delivering nano-metallic alloys to infected cells in a patient is disclosed. The nano-metallic alloy may be formed from binary, triple, or quadruple elemental compositions complexed in predetermined percentages of monosodium phosphate monohydrate and disodium phosphate heptahydrate. The nano-metallic alloy may be capable of eliminating infectious microorganisms within infect cells or legions without harming the cells or tissues. The system may also include a method of administering a predetermined concentration of the nano-metallic alloy in the complexing solution in the vicinity of the infected cells of legions to kill the foreign matter.
US20090291909 Aminosugar, glycosaminoglycan, and s-adenosylmethionine composition for the treatment and repair of connective tissue A composition for the protection, treatment and repair and for reducing the inflammation of connective tissue in mammals and a method for the treatment of connective tissue in mammals by the administration of the composition. The composition includes S-Adenosylmethionine (SAM), and a component selected from an aminosugar or salts thereof (e.g., glucosamine) or glycosaminoglycans (e.g., chondroitin salts) or mixtures or fragments thereof. The composition optionally includes manganese which promotes the production of connective tissue matrix. The composition also optionally includes methyl donors or methyl donor cofactors, such as vitamin B12, vitamin B6, folic acid, dimethylglycine or trimethylglycine.
EP1359920B1 Uses of oral formulations for the treatment of female sexual dysfunction A pharmaceutical composition for the treatment of sexual dysfunction, particularly post-menopausal females, is provided. The composition includes a therapeutically effective amount of an estrogenic compound, androgenic compound, vasodilation compound, and a pharmaceutically acceptable carrier.
CN103285007A Application of Myriberine A in preparation of acute gout treatment drug The present invention provides a new use of Myriberine A in medicine, specifically an application of the Myriberine A in preparation of an acute gout treatment drug. Experimental research results show that the Myriberine A provides a protection effect for an acute gout model with human vascular endothelial cell damage caused by urate, and can be provided for inhibiting ICAM-1 expression, such that the Myriberine A can be used for preparing the acute gout inflammation treatment drug. According to the present invention, the use of the Myriberine A in acute gout treatment drug preparation is firstly disclosed, the skeleton belongs to a completely-new skeleton type, acute gout prevention and treatment activity of the drug is strong, possibility that any revelation is provided by other compounds does not exist, the drug has prominent substantive characteristics, and significant progress is provided for acute gout prevention and treatment with the drug.
US20080318918 Methods for Treatment and Prevention of Otitis Media Using Nonionic Surfactants to Facilitate Transmembrane Drug Delivery into the Middle Ear Methods for treating and preventing middle ear infections by transmembrane administration of medicament-containing transmembrane carrier compositions comprising a nonionic polymer surfactant, such as an alkyl aryl polyether alcohol (e.g., tyloxapol) to the tympanic membrane. The medicaments delivered according to the methods of the invention include antibiotic, antiviral, anti-fungal and anti-inflammatory agents that are useful in treatment and/or prophylaxis of middle ear infections and their sequelae.
WO2006075690A1 Stable medicinal composition To provide a stable medicinal composition containing an EP4 agonist. An aqueous solution containing a dextrin clathrate of methyl 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3(methoxymethyl)phenyl]but-1-enyl}-5-oxocyclopentyl)ethyl]sulfanyl}butanoate, which has EP4 agonistic activity, is mixed with a sugar and optionally with a pH adjustor to regulate the pH to about 3-6.5. The mixture is then freeze-dried. The freeze-dried product obtained is stable during storage and generates no decomposition products. It is hence usable as a higher-quality preparation for injection in clinical practices.
US20100298342 Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's Disease The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
CN100581539C Effective component of hedyotis diffusa and method of preparing the same and application The invention provides the effective constituents of oldenlandia, which mainly contain two compounds of 2-methoxyl-3-hydroxyanthraquinone (A) and 2-methyl-3-hydroxyanthraquinone (B), wherein the content of A is 55-75%, the content of B is 15-25%. The constituents are obtained through steps of heating, extracting, concentrating, separating with silica gel column, eluting, concentrating and drying the eluent, continuously conducting liquid phase chromatographic separation, collecting the solution, concentrating and drying the solution. The effective constituents can be used for treating and preventing tumors.
WO2012074440A3 Pharmacological composition intended for intra-nasal administration with the aim of supplying a pharmacologically active component to the brain, and method for producing said composition The claimed group of inventions relates to the field of pharmacology and medicine. The pharmacological composition is intended for intra-nasal administration and enables an active substance to be supplied directly to the brain, by-passing the blood-brain barrier. The composition comprises a base container, a pharmacologically active component and a surface-modifying substance. Porous particles of an inorganic substance are used as the container, and the surface of the container is modified with surfactants, polymers or with a combination thereof. The containers made of an inorganic substance have a size in the range from 300 to 5000 nm. Inorganic substances selected from a group consisting of metal salts or oxides, for example calcium carbonate or titanium oxide, in the form of porous particles of a micron or sub-micron size, are used as the base container. For the surface-modifying substance, use is made of surfactants selected from polysorbates, or of polymers, selected from a group consisting of glycosaminoglycans, polypeptides, or combinations thereof. The method for producing the designated composition comprises producing the base container, sorbing the pharmacologically active substance in volumes of the pores in said container, and modifying the surface of said container. The base container is synthesized from inorganic substances in the form of porous particles of a micron or sub-micron size, and the surface of the designated particles of the base container is additionally modified with polymers selected from the group consisting of glycosaminoglycans or polypeptides, or with surfactants selected from the group consisting of polysorbates, or with combinations thereof.
CN103027954A Self-making method of household lithospermum oil The invention discloses a self-making method of household lithospermum oil. The formula is composed of the following components by weight: 200 ml of olive oil, 50 g of lithospermum and 5 g of borneols. The olive oil is sweet and cool and is easily absorbed by the skin, is pure in taste and is also suitable for brewing; the lithospermum is sweet and salty-cold and the borneol is bitter and slightly cold, and the two materials together achieve the effects of cooling blood, invigorating the circulation of blood, detoxifying, clearing heat and relieving pain and removing slough and promoting growth of tissue regeneration. The lithospermum oil is a pure plant preparation which is very mold without stimulation to the skin; and the materials and the method both are simple and household making is convenient. The household lithospermum oil is suitable for preventing and treating red butt, diaper rash and the like of babies.
CN101406689A Method for producing liver-boosting capsule containing glutathione and other nine ingredients The invention discloses a method for producing a Jiugantai liver-nourishing capsule, which belongs to the technical field of food processing, in particular to a processing technology of health care food. The invention aims to provide a Jiugantai capsule processing method with high practical value and good combination effect to enter industrialized production. The technology adopted by the method is characterized in that the content of an active ingredient, namely glutathione can be controlled to achieve steady quality. The Jiugantai capsule produced by the technology is a nutritional capsule consisting of nine ingredients such as the glutathione and vitamins and so on. The Jiugantai capsule has the following advantages: (1) the capsule is a special nutritional capsule and is a good friend of livers; (2) the utilization of the quality control of the glutathione and the vitamin are favorable for a product to enter international market; and (3) the product has long guarantee period, steady ingredients, convenient administration, and feasibility. The product also contains pollen polysaccharide, vitamins, amino acid, and various trace elements which are necessary to human bodies, has health care function of promoting the immunity of organisms, and particularly has important significance on fatty liver and hepatic injury, so the product has broad market prospect.
CN103159774A Extraction, separation and purification method for strychnos total alkaloid The invention discloses an extraction, separation and purification method for strychnos total alkaloid, and belongs to the technical field of medicines. The method comprises but is not limited to the following steps of: treating strychnos coarse powder via an acid water extraction-organic solvent extraction method or an alkalization-organic solvent extraction method or an alcohol extraction-organic solvent extraction method to obtain the strychnos total alkaloid; purifying the total alkaloid via a solvent-stepwise extraction method or a column chromatography method or a hydrochloride-sulphate stepwise crystallization method; and then preparing via the hydrochloride-sulphate stepwise crystallization method or the column chromatography method to obtain strychnine having a purity of greater than 90%.
WO2011104568A1 Treatment of oxidative stress disorders The use, in the treatment or prevention of ocular lens degeneration, corneal degeneration, skin degeneration or any ROS-induced degeneration of other tissues or organs characterised by the ER stress response, or in the preparation of a medicament for such degeneration treatment or prevention, of an active therapeutic agent comprising one or more sigma 1 receptor agonist.
US20120316227 Chrysophaentin antimicrobial compounds that inhibit ftsz protein Embodiments of antimicrobial chrysophaentin compounds, pharmaceutical compositions including the chrysophaentin compounds, and methods for using the chrysophaentin compounds are disclosed. Some embodiments of the disclosed compounds are isolated from Chrysophaeum taylori. Certain embodiments of the chrysophaentin compounds inhibit FtsZ protein, thereby inhibiting the growth of clinically relevant bacteria, including drug-resistant strains.
CN1737007A Gastrodine derivative, its preparation method, pharmaceutical composition and uses The invention relates to a gastrodine derivative, its preparing process, pharmaceutical compositions containing it and the use as medicament. More specifically, the derivative has an English name of 4-(acetoxymethyl)phenylglucoside.
EP1565182A1 Treatment of gastrointestinal disorders with duloxetine The present invention belongs to the fields of medicinal and pharmaceutical chemistry, and provides a new method of treating gastrointestinal disorders by the administration of duloxetine.
CN101628067B Medicament for treating diskal hernia and arthralgia The invention discloses a medicament for treating diskal hernia and arthralgia, which is a reagent prepared from the following raw materials according to the weight ratio: 25 to 65 portions of pendulous monkshood root, 25 to 65 portions of Chinese alangium root, 25 to 65 portions of crispateleaf ardisia root, 25 to 65 portions of common claoxylon root and leaf, 25 to 65 portions of corydalis tuber, 25 to 65 portions of paniculate swallowwort root, 25 to 65 portions of scandent schefflera stem and leaf, 25 to 65 portions of clematis root, 25 to 65 portions of garden balsam stem, 25 to 65 portions of pubescent angelica root, 25 to 65 portions of dahurian angelica root, 25 to 65 portions of yam, 25 to 65 portions of shinyleaf pricklyash root, 20 to 50 portions of red psychotria branchlet andleaf, 20 to 50 portions of solanum lyratum, 20 to 50 portions of rhizoma typhonii, 20 to 50 portions of bostonivy, 20 to 50 portions of henry magnoliavine stem or root, 20 to 50 portions of philippine flemingia root, 20 to 50 portions of asarum, 20 to 50 portions of sarcandra, 20 to 50 portions of rose mallow root, 20 to 50 portions of Chinese starjasmine stem, 20 to 50 portions of Asiatic toddalia root, 100 to 150 portions of camphor, 2,500 to 3,500 portions of medical ethanol, and 500 to 1,200 portions of dimethyl sulfoxide. The medicament has a reasonable formula, and has remarkable therapeutic effect through the clinical case statistics. The medicament can synchronously have well therapeutic effect on the diskal hernia and the arthralgia.
EP2601191A2 Compounds and compositions for mitigating tissue damage and lethality Embodiments of the present invention provide compounds and compositions thereof, which are effective for mitigating tissue damage or lethality induced by an agent, and methods of making and using the same.
CN102872011A Pharmaceutical composition comprising (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide The invention relates to a pharmaceutical composition comprising (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide. Particularly, the invention relates to a pharmaceutical composition comprising levorotatory (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide, which comprises active components and pharmaceutically acceptable auxiliary materials. The pharmaceutical composition of the invention has good properties.
CN103393665A Application of Sarcaboside A to medicament for treatment of renal carcinoma The invention discloses application of Sarcaboside A to preparation of medicaments for the treatment of renal carcinoma and belongs to the technical field of novel application of medicaments. Through in vitro MTT antineoplastic activity evaluation, it is discovered that Sarcaboside A has substantial inhibition effect on growth of a human renal carcinoma cell strain KC. Accordingly, the Sarcaboside A can be applied to the preparation of medicaments for resisting renal carcinoma and has good development and application prospects. The application of Sarcaboside A to the preparation of medicaments for the treatment of renal carcinoma involved in the invention is disclosed for the first time. The Sarcaboside A has a novel skeleton type and unimaginably strong activity in inhibition of renal carcinoma cells.
WO2010035766A1 Method for producing triazole derivative Provided is a method whereby a triazole derivative having a (1,3-dioxan-5-yl)thio group of improved qualities can be produced at an elevated yield by using an industrially more advantageous operation while reducing impact on the environment. Also provided is a triazole derivative having a high purity. Sodium hydroxide or sodium ethoxide is used in a reaction between an epoxide and a thioester. Hydrochloride of a diol compound is reacted with an aldehyde in the presence of trimethylsilyl chloride together with an organic base and in the presence or absence of an alcohol. Further, sodium methoxide is used in a coupling reaction between a phosphonic acid ester and an aldehyde.
US7261888 Combined use of triglycerides containing medium chain fatty acids and exogenous lipolytic enzymes as feed supplements The present invention relates to the use of triglycerides (TG) containing medium chain fatty acids (C4 to C12), combined with exogenous lipolytic enzymes (esterases or lipases) as a feed supplement for animals in order to prevent and/or alleviate the problems which are frequently met at this moment. This results in a marked improvement of the growth performances without the use of the classical, but contested, feed additives.
WO2013137495A1 Replication competent pseudo-type retrovirus vector system The present invention can insert a therapeutic gene into both of vectors of a vector system in which the MuLV-Gag gene, the MuLV-Pol gene, and the GaLV-Env gene are divided into two vectors so as to be expressed, and thus it is possible to insert various foreign genes for therapy so as to safely and effectively transfer the same to a target cell tissue region of abnormal proliferation without a restriction on the size of the gene to be inserted. Therefore, it is possible to use: a composition, which contains a retrovirus produced by transfecting cell lines with the vector system, for transferring a gene targeting a cell of abnormal proliferation which abnormally divides; and a composition for preventing or treating diseases causing a cell of abnormal proliferation, such as cancer.
EP1891057B1 Azabicyclo[3.1.0]hexane derivaives as dopamin d3 receptor modulators The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: (I), processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
CN1846673A Slow-released anticancer medicine prepn containing pyrimidine medicine The slow released anticancer injection consists of slow released microballoon and solvent. The slow released microballoon includes effective anticancer component and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The effective anticancer component includes pyrimidine analogue and pyrimidine analogue synergist of phosphorinositide 3-kinase inhibitor and/or DNA repair enzyme inhibitor; the slow releasing supplementary material is PLA, PLGA, EVAc, etc or their composition; and the suspending agent is sodium carboxymethyl cellulose, mannitol, sorbic alcohol, Tween-80 or their composition. The slow released microballoon may be also prepared into slow released implantation preparation. Implanting or injecting the slow released preparation to local tumor part can lower the systematic toxic reaction of the medicine and raise the medicine concentration of local tumor part selectively to raise the treating effect.
CN103242286A Bicyclol medical composition and preparation method thereof The invention relates to a bicyclol medical composition and a preparation method thereof. The composition is composed of bicyclol and a structural compound shown in Formula II. The invention further separates, purifies and characterizes the structure and activity of bicyclol related substances, and proves that a substance causing abnormal hemoglobin and leucocyte counting and other adverse reactions is the structural compound shown in the Formula II. The preparation method provided by the invention ensures that the safety and stability of the bicyclol medical composition are improved. The Formula II is shown in the specification.
EP1499312B1 The use of hydroxypyridone-derivatives in wound healing The present invention relates to the use of compounds of the formula (I), in which R<1>; R<2>; R<3> and R<4> have the meanings indicated in the claims, for the treatment of wound healing.
CN1810256A Policresulen foam aerosol and its prepn process The present invention discloses one kind of policresulen foam aerosol. The policresulen foam aerosol has softness, fineness, no excitation, excellent adsorption, excellent expansion and other advantages, can penetrate to mucous membrane goffer and other parts common medicine preparation can not reach to, and is suitable for use in body cavity. Clinic application shows that the policresulen foam aerosol is superior to corresponding spraying agent in treating cervicitis and vaginitis. The present invention also provides its preparation process.
US20090306051 Methods and compositions for the treatment of epilepsy, seizure disorders, and other CNS disorders The present invention relates to methods and compositions for treating CNS-related disorders.
CN102813645A Control effect and mechanism of mangiferin on diabetic encephalopathy The invention relates to novel pharmacologic action of mangiferin, i.e., effects of mangiferin on preventing and treating diabetic encephalopathy. Mangiferin can obviously improve cognitive impairment caused by diabetes, remarkably reduce the level of advanced glycation endproducts (AGF) in the brain and expression of the acceptor RAGE thereof, substantially enhance activity and expression of glyoxalase 1 (Glo-1) in the brain, remarkably reduce the level of interleukin 1-beta (IL-1beta) and tumor necrosis factor alpha (TNF-alpha) in the brain, substantially improve the level of reduced glutathione (GSH) in the brain, remarkably reduce the level of malonaldehyde (MDA) in the brain, substantially improve the activity of superoxide dismutase (SOD) and the level of GSH in serum and substantially reduce the level of MDA in the serum. Mangiferin can be used for preventing and treating diabetic complications like diabetic encephalopathy.
US7884109 immunosuppressants such as 2-(6-Fluoro-1H-benzo[d]imidazol-1-yl)-9-((1R,4R)-4-hydroxy-1,2,3,4-tetrahydronaphthalen-1-yl)-7H-purin-8(9H)-one, used for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulas:
CN102197023A Compounds for treating ophthalmic diseases and disorders Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
CN102772420A Swine bile phthalate eye drops and preparation method thereof The invention discloses swine bile phthalate eye drops, consisting of the following compounds in percentage by weight: 0.1%-3% of swine bile phthalate, 0.1%-5% of thickening agent, 0.6%-0.85% of sodium chloride, 0.01%-0.1% of ethyl-para-hydroxybenzoate, and the balance of water for injection; and the thickening agent is one or more of sodium hyaluronate, methylcellulose and carbomer. Moreover, the invention further discloses a preparation method of the eye drops. According to the bile phthalate eye drops, swine bile phthalate is used as a main compound for preparing the swine bile phthalate eye drops according to the preparation requirement of eye drops; the preparation technology is simple and reasonable; the prepared eye drops is stable in performance, safe and reliable, has antivirus and anti-inflammatory effects, and is used for clearing heat and detoxicating, calming the liver and improving eyesight, and treating viral keratitis and conjunctivitis caused by liver-fire flaming and hot eye hurting symptoms; and the product has the characteristics of determined curative effect, little toxic or side effect, little irritation, and the like, and is suitable for clinical application and industrial large-scale production.
CN103664892A Crystal of quinoline derivative The invention relates to a crystal of a quinoline derivative, a preparation method of the crystal, a pharmaceutical composition comprising the crystal and application of the pharmaceutical composition in the field of medicine, in particular to three crystalline solid manners of quinoline derivative dihydrochloride, namely an A-type crystal, a B-type crystal and a C-type crystal, wherein the A-type crystal and the B-type crystal are crystals basically not containing crystal water molecules and other solvents, and the C-type crystal is the crystal containing two crystal water molecules.
US20060057219 Method for preparing a polymer micelle pharmaceutical preparation containing drug for injection A production method of a preparation containing drug-encapsulating polymer micelles is provided, which comprises dissolving a hydrophilic-hydrophobic block copolymer and a sparingly water-soluble drug in a volatile organic solvent, then removing the solvent, and stirring the residue with water at a temperature not higher than 30° C. to dissolve the drug-encapsulating polymer micelles into the water.
WO2007099869A1 Therapeutic and preventive agent for hcv The inventors of this application carried out an investigation of the HCV replicon inhibitory activity of U18666A and found that the compound has an effect on inhibiting the replication of HCV replicon RNA or the expression of HCV protein. Further, when the inventors carried out a knockdown experiment of DHCR24 using siRNA, it was found that the HCV replicon activity and HCV protein expression are significantly inhibited in a cell in which DHCR24 expression is suppressed. Base on these findings, it was revealed that HCV infection can be treated or prevented by inhibiting an enzymatic activity related to the process of cholesterol biosynthesis.
CN1887262A Slow released anticancer medicine injection containing bendamustine and its synergist The slow released compound anticancer injection containing bendamustine and its synergist consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is the composition of bendamustine and bendamustine synergist selected from phosphoinositide 3-kinase inhibitor, pyrimidine analog and DNA repairase inhibitor. The slow releasing supplementary material is polylactic acid and its copolymer, polifeprosan, EVAc or other biocompatible polymer. The .suspending agent is carboxymethyl cellulose, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent. The present invention can inhibit the growth of tumor and enhance the curative effect of chemotherapy, radiotherapy and other non-operative treatment.
US6872720 Pyrazolo-triazine derivatives as ligands for gaba receptors A class of substituted pyrazolo[1,5-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 7-position, an alkyl group at the 4-position, and a substituted alkoxy moiety at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
US20100273734 Derivatives of Hyaluronic Acids The present invention relates to methods for preparing a derivative of a hyaluronic acid, comprising: (a) mixing a liquid solution comprising the hyaluronic acid and a diamine, a polyamine, or a combination thereof, at a pH suitable to form an imine; (b) reducing the imine to an amine with a reductant at a pH suitable to produce the derivative of the hyaluronic acid; and (c) recovering the derivative of the hyaluronic acid. The present invention also relates to isolated derivatives of a hyaluronic acid, comprising the hyaluronic acid and a diamine, a polyamine, or a combination thereof.
CN1569029A Medicine for treating recurrent psoriasis and its preparing process The invention provides a medicament for treating tinea, which comprises arsenic trioxide AS2O3, borneol, auxiliary ageng sodium hydroxide, hydrochloric acid and balancing distilled water.
CN1857301A Composition for matching with contact lenses and its application The present invention relates to a kind of composition for use matching with contact lenses and its application. The composition contains amino acid polymer, inosine and vitamin B6 eye drop, and can lubricate contact lenses and eyes, protect eyes and make wearing of contact lenses comfortable. It is dropped into eyes while the contact lenses are in.
US7368469 Prophylaxis of stroke, cardiovascular death or myocardial infarction by administering an angiotenzin converting enzyme inhibitor: ramipril, ramiprilat or their salts, optionally together with another antihypertensive, a cholesterol lowering agent, a diuretic or aspirin Use of an inhibitor of the renin-angiotensin system or a pharmaceutically acceptable derivative thereof, optionally together with another antihypertensive, a cholesterol lowering agent, a diuretic or aspirin, in the manufacture of a medicament for the prevention of cardiovascular events; a method of preventing cardiovascular events comprising administering to a patient in need of such prevention an effective amount of an inhibitor of the renin angiotensin system or a pharmaceutically acceptable derivative thereof, optionally together with another antihypertensive, a cholesterol lowering agent, a diuretic or aspirin; and a combination product containing an an inhibitor of the renin-angiotensin system or a pharmaceutically acceptable derivative thereof and a cholesterol lowering agent.
WO2010012131A1 The usage of medicinal composition containing oil of zedoary turmeric in manufacture of medicaments The usage of medicinal composition containing oil of zedoary turmeric and borneol in manufacture of medicaments for preventing and treating diseases such as virus infection of HPV, cerbical intraepithelial neoplasia, papilloma, cervical carcinoma, etc., in particular diseases infected by high risk HPV. The medicinal composition may be made into all kinds of dosage forms, and can play an important role in preventing and treating the related diseases of a great variety of virus infection of HPV.
CN1634112A Azithromycin gel formulation and its preparing process The invention relates to an Azithromycin gel formulation and its preparing process, which is a gel form oral administration preparation prepared through using Azithromycin and right amount of base material as gel or paste, the aged people and children are willing to take the preparation. The preparation can be used for treating respiratory tract, skin and soft tissue affection diseases caused by responsive microorganisms. The invention also provides the process for preparing the preparation.
US20080108697 Using a glass bottle containing oxaliplatin in aqueous solution at a concentration between 2 mg/ml and 7 mg/ml; metastatic colorectal cancers; surface/volume ratio of the flask, expressed in mm2/mm3, is less than 0.26 The invention concerns an assembly consisting of an aqueous oxaliplatin solution and a glass flask containing same, characterised in that the surface/volume ratio of the flask, expressed in mm2/mm3, is less than 0.26.
CN101747272B Crystal form B of blonanserin and preparing method thereof The invention provides a crystal form B of medicament 2-ethylpiperazine-4-(4-fluorobenzene)-5,6,7,8,9,10-hexahydro cyclooctane pyridine, which is characterized in that powder diffraction occurs in the positions of approximately 7.74+/-0.2, 15.6+/-0.2, 19.1+/-0.2 and 31.64+/-0.2 of a reflecting angle 2 theta through X-ray. The invention also provides a preparing method of the crystal form B, whichis characterized by comprising the following steps of: ensuring that the medicament 2-ethylpiperazine-4-(4-fluorobenzene)-5,6,7,8,9,10-hexahydro cyclooctane pyridine is dissolved in ethanol by heating, and then obtaining the crystal form B through recrystallization.
EP2399611A2 Use of an oligonucleotide or its active derivative for the preparation of a pharmaceutical composition for inhibiting the formation of metasatases in cancer treatment The present invention is related to pharmaceutical compositions for the inhibition of metastases and treatment of cancer such as bladder carcinoma, colon cancer, endometrial cancer, hepatocellular carcinoma, leukemia, lymphoma, melanoma, non-small cell lung cancer (NSCLC), ovarian cancer, pancreatic cancer, prostate cancer, soft tissue cancer, renal cancer, osteosarcoma, mesothelioma, myeloma multiple, bladder carcinoma and esophagcal cancer as well as the use of these pharmaceutical compositions for the treatment of said metastases and cancers. Another aspect of this invention are new antisense oligonucleotides inhibiting the formation of human interleukin 10 and their synthesis. A further aspect of this invention is the use IL-10 antisense oligonucleotides for the preparation of pharmaceutical compositions and for the treatment of cancer and metastases.
CN103230008A Health care food with weight losing function and preparation method of food The invention discloses a health care food with a weight losing function and a preparation method of the food. The health care food is formed from the following raw materials: bighead atractylodes rhizome, hawthorn, lotus leaves, rhizoma alismatis, semen cassiae, L-carnitine and starch. The preparation method comprises the following steps of: digesting the bighead atractylodes rhizome, hawthorn, lotus leaves, rhizoma alismatis and semen cassiae for pulverizing, preparing a mixture of the L-carnitine and the starch; and blending, pelletizing, metering for dividing, and packaging. The product obtained through the process is safe to take, has an obvious health care effect, and also is low in industrial production cost.
WO2009053550A1 Rimonabant n-methylpyrrolidone solvate, method for preparing same and pharmaceutical compositions containing same The invention relates to a rimonabant N-methylpyrrolidone solvate, to a method for preparing the same and to the therapeutic uses thereof.
CN103079550A N-acetyl-DL-leucine, neuroprotective and retinoprotective medicament The invention relates to a medicament, the active principle of which is a leucine and, for example, a N-ACETYL-DL-LEUCINE. It can be applied to the prevention and/or treatment of eye diseases or disorders and especially of hereditary dystrophies of the retina, glaucomatous neuropathy, glaucoma, macular degeneration, myopia, presbyopia, hypermetropia, astigmatism, all the ophtalmologic diseases or disorders inducing a decrease of visual function and/or age-related physiological vision decline.
EP1406613B1 Organic nitratederivatives for the treatment of atherosclerosis and vascular diseases Use for the vasculopathy treatment of compounds or salts thereof, having the following general formula: A-(B)b0-(C)c0-NO2 wherein A is the radical of the precursor drug selected between the salicylic or acetylsalicylic acid, B and C are bivalent linking groups as defined in the invention.
US8618141 Aryl ureas with angiogenesis inhibiting activity This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.
US20090093547 Compositions and Methods for Treating Premature Ejaculation Compositions and methods for the treatment of premature ejaculation have been developed. It has been discovered that premature ejaculation can be treated by administering a local anesthetic to the glans penis. The local anesthetic may be formulated as an emulsion, lotion, paste, gel, cream, ointment, shea butter, suspension, solution, balm, salve, foam, or in the form of a pump spray to achieve local anesthesia of the dorsal neurons of the penis.
WO2013133221A1 micro-RNA INHIBITOR Provided is a micro-RNA inhibitor which has broad utility and is rarely decomposed. A micro-RNA inhibitor (1) characterized by having at least two complementary sequences (2) to the sequence for micro-RNA to be inhibited, wherein the at least two complementary sequences (2) are linked to each other through a linker residue (3).
CN102203074A Aryl GPR119 agonists and uses thereof Aryl GPR119 agonists are provided. These compounds are useful for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control.
CN1813804A External-use ointment and its preparing method The present invention discloses a kind of six spirits ointment for external application, including six spirits adhesive plaster, six spirits rubber plaster, six spirits babu preparation and six spirits ointment. It is made up by using six spirits pill powder as main medicine and adding matrix through a certain preparation process, and has the functions of clearing away heat and toxic material, relieving inflammation and stopping pain and can obtain good therapeutic effect for curing furuncle in children, large carbuncle, acute mastitis, innominate inflammatory swelling, herpes and mammitis, etc.
CN103748079A Pyridazinone compounds and their use as DAAO inhibitors The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, wherein R1 and R2 are as defined in the specification
EP1776368A1 Inhibitors of hcv replication Indole compounds of Formula (I) are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.
US7351422 Hemostatic soluble cellulose fibers containing coagulating protein for treating wound and process for producing the same Proposed is a novel soluble trauma-healing and hemostatic cellulose fiber capable of absorbing and readily dissolving hemorrhaging trauma loci when applied thereto and of promoting the hemostatic action of blood platelets and fibrin and cell adhesion to the trauma site. The coagulation protein-containing soluble trauma-healing and hemostatic cellulose fiber is produced in that after treatment of a natural or regenerated cellulose fiber with an aqueous sodium hydroxide solution, said fiber is carboxymethylated by reaction with a monochloro acetic acid solution for a given time (hours) in such a manner that the degree of partial substitution of the glucose units constituting the cellulose molecule (etherification degree) is 0.5-less than 1.0% and that, furthermore, the coagulation proteins fibrinogen, thrombin, and coagulation factor XIII are imparted by surface application or chemical bonding.
CN1771954A Vinorelbine liposome micro ball injection and its prepn The present invention relates to one kind of vinorelbine liposome micro ball injection and its preparation process. The present invention has vinorelbine medicine in 90-98 % coated inside the oil phase and oil-water interface of liposome micro ball, reduces the clinical toxicity and irritation of vinorelbine greatly and raises its antitumor effect. The preparation of the present invention as one kind of antitumor injection has low irritation, low toxicity and high curative effect.
EP0944592B1 Vitamin d3 derivatives A compound of formula (I) in which formula Q is a C1-C6 hydrocarbylene diradical; Y is either a single bond, a carbonyl group or a methylene, ethylene, -CH(OH)-, -O-(C6H4)- (ortho, meta, para) or -S-(C6H4)- (ortho, meta, para) diradical; R?1 and R2¿, which may be the same or different, stand for hydrogen or a C¿1?-C6 hydrocarbyl radical; or R?1 and R2¿, when taken together with the carbon atom (starred in formula I) bearing the group Z, can form a C¿3?-C6 carbocyclic ring; and Z is hydrogen or hydroxy; with the proviso that when, at the same time, Q is ethylene, Y is methylene, R?1 and R2¿ stand for methyl or trifluoromethyl, and Z is hydroxy, or when, at the same time, Q is ethylene, Y stands for carbonyl or -CH(OH)-, R?1 and R2¿ are methyl, and Z is hydroxy, then the configuration at C-20 cannot be E. The compounds show anti-inflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells.
CN101862305A Ambroxol hydrochloride sustained-release pellet and preparation method The invention relates to the composition of an ambroxol HCl-containing sustained-release pellet and a preparation method. The sustained-release pellet consists of two parts which are a quick-release pellet core and a sustained-release coating film respectively, can achieve the effect of long-term release approaching to zero-order release, is mainly used for treating acute and chronic respiratory diseases, and is a medicament of first choice for dispelling phlegm.
US6881730 Steroid compounds with a c17-alkyl side chain and an aromatic a-ring for use in therapy Compounds of Formula (I) in which: R1 and R2, which may be the same or different, each represents a lower alkyl, alkenyl or alkynyl group; R3 represents a methyl group having α- or β-configuration; R4 represents a hydrogen atom or an etherifying or esterifying group; R5 represents a hydrogen atom, a hydroxyl group or a lower alkoxy group; X represents a group OR4, wherein R4 is as defined above, or a group NR6R7 wherein R6 represents a hydrogen atom, an aliphatic or araliphatic organic group, or an acyl group comprising an aliphatic, araliphatic or aryl organic group linked to the nitrogen atom by way of a carbonyl group; and R7 is a hydrogen atom or a lower alkyl group; Y represents a lower alkylene, alkenylene or alkynylene group optionally substituted by a hydroxyl, etherified hydroxyl or esterified hydroxyl group; and the dotted lines signify that double bonds may be present at the 16(17)-position and/or either at the 6(7)- and 8(9)-positions or at the 7(8)-position exhibit potent effects on modulation of cell growth and differentiation, while having low calcaemic activity.
CN101711756B Application of 3-phenyl-3-(4-nitryl phenylamino)-1-(4-chlorphenyl)-1-acetone as non-steroidal androgen receptor regulating agent The invention belongs to the field of pharmaceutical chemistry, in particular to an application of 3-phenyl-3-(4-nitryl phenylamino)-1-(4-chlorphenyl)-1-acetone with the following structural formula as a non-steroidal androgen receptor regulating agent. The compound has an androgen receptor antagonist and is a medicament for preventing or/and treating symptoms or diseases of prostatic hypertrophy, prostatic cancer, hirsutism, serious androgen dependent alopecia or acne, and the like.
CN102100670A Poly(lactic-co-glycolic acid) nanoparticle, preparation method and application thereof The invention belongs to the field of biomedicines, and more particularly discloses a poly(lactic-co-glycolic acid) nanoparticle internally covering taxol and externally connecting a humanized SM5-1 antibody, a preparation method and application thereof. The poly(lactic-co-glycolic acid) nanoparticle internally covering taxol and externally connecting a humanized SM5-1 antibody, disclosed by the invention, has the characteristics of excellent biologic targeting performance and remarkable function of in-vitro killing target tumor cells, and can be used for preparing medicines capable of treating tumor with p230 antigens high expression.
WO2005018557A3 Substituted pyridinones Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
CN103435714A Preparation and purification methods and application of fig crude polysaccharide The invention discloses a preparation method of fig crude polysaccharide, which comprises the following steps: taking dried fig, pulverizing, refluxing with 95% ethanol to remove grease and pigments, carrying out vacuum filtration, and refluxing the residues with 70% ethanol to remove small molecule impurities; taking the residues as the raw material for extracting fig polysaccharide; and taking the residues, extracting under microwave conditions by using water as a solvent, carrying out vacuum filtration, concentrating the filtrate to 100Ml by rotary evaporation, adding 95% ethanol, standing for 24 hours, centrifugating, taking the precipitate, removing proteins from the precipitate by a Sevage process, and carrying out freeze-drying to obtain fig crude polysaccharide. In the extraction process, the ratio of the residues to the water is 1:(20-23), the microwave power is 550W, and the extraction time is 13 minutes; and the ethanol for alcohol precipitation is 3.50-3.60 times by volume of the extracting solution. The invention also discloses a purification method and application of the fig crude polysaccharide.
WO2012171065A1 Treatment of allan-herndon-dudley syndrome with 3,5-diiodothyropropionic acid (ditpa). The present invention relates to pharmaceutical compositions comprising DITPA, and methods and uses of the pharmaceutical compositions for the treatment for Allan-Herndon-Dudley syndrome including a dosage regime.
CN101234120A Notoginseng dropping pills and preparation method thereof A Sanqi drop-pill is composed of the following components with the following weight proportions: 20-30 percent of polyethylene glycol 4,000, 40-55 percent of polyethylene glycol 6,000 and 25-30 percent of panax notoginseng saponins. The preparation steps are as follows: first heating the polyethylene glycol 6,000 for completely melting, stopping heating when the temperature is risen to 75-85 DEG C and carrying out heat preservation; adding in panax notoginseng saponins and mixing well for completely melting into the polyethylene glycol 6,000; then adding in polyethylene glycol 4,000, heating and keeping the temperature between 75 DEG C and 85 DEG C; stirring for 15-25min for well mixed of panax notoginseng saponins and polyethylene glycol; drop processing the Sanqi drop-pills. The Sanqi drop-pill of the invention has the advantages of easy administration, complete absorption and good effect, while the preparation method of the invention is simple in operation, easy to master, low in cost and of no loss of nutrition components in the product preparation process.
CN101919837A Application of rosmarinic acid in preparing medicament for treating or preventing renal fibrosis The invention provides application of rosmarinic acid in preparing medicament for treating or preventing renal fibrosis. The medicament can be of oral administration and injecting administration, wherein the dosage in injecting administration is between 50 and 1,500mg; and the dosage in oral administration is between 100 and 3,000mg.
US7838510 Biomaterials based on hyaluronic acid for the anti-angiogenic therapy in the treatment of tumors The use in the medical-surgical field of biomaterials based on hyaluronic acid derivatives, optionally in association with natural, synthetic or semisynthetic biopolymers, for suppressing the angiogenic process associated with tumor proliferation (in primary and secondary tumors) is disclosed.
US20090264456 Compostions and methods for preventing and/or treating disorders asociated with cephalic pain Compounds, e.g., of formula (I) and (Ia), pharmaceutical compositions comprising the compounds and methods of using the compounds and pharmaceutical compositions for treating pain disorders, e.g., disorders associated with cephalic pain, are provided.
CN102018216A Composition containing bifidobacteria for adjusting intestinal flora and enhancing immunity A composition containing bifidobacteria for adjusting intestinal flora and enhancing immunity is characterized by comprising, by weight, 0.01-10% of bifidobacteria, 10-50% of oligosaccharide, 0.01-10% of vitamin, and 0.01-10% of metals, with the balance being auxiliary materials. The composition containing bifidobacteria provided by the invention has functions of adjusting intestinal flora and enhancing immunity. The composition can be made into capsules, soluble granules, granules, tablets, etc., and applied in food, health product and pharmaceutical fields.
US20090075327 Methods for improving secondary metabolite production in fungi The invention relates to the production of secondary metabolites by fungi. More particularly, the invention relates to improvement of production of commercially important secondary metabolites by fungi. The invention provides methods for improving secondary metabolite production in a fungus, comprising modulating the expression of a gene involved in regulation of secondary metabolite production.
WO2010081104A1 Use of polymeri zable quaternary ammonium compounds to inhibit endogenous mmps in tooth dentin Disclosed are compositions and methods of using such compositions for inhibiting matrix metalloproteinase activity in dental tissue. The compositions, methods and uses may prevent degradation of the bonding between restorative materials and dental tissues, thereby increasing durability and longevity of the restorative material-dental tissue bonds. For example, the compositions, methods, and uses of the present invention may be used for treating carious dental tissue such as by the creation of dental fillings, crowns, bridges, among other techniques, as well as the creation of esthetic laminate restorations.
US20050037462 Expression vector comprising nucleotide sequences coding g protein for use in generating immunoglobulins for use in prevention, treatment and diagnosis of cell proliferative disorders The present invention provides an isolated nucleic acid molecule whose sequence encodes the amino acid sequence for gp75 or a fragment thereof. The present invention further provides an isolated cDNA molecule of the gp75 nucleic acid molecule or a fragment thereof and the amino acid sequence derived therefrom. This invention also provides vaccines for stimulating or enhancing in a subject to whom the vaccine is administered production of antibodies directed against gp75. This invention further provides methods using the vaccines of this invention for stimulating or enhancing production of antibodies against gp75 as well as for treating, preventing or delaying the recurrence of cancer.
US20110105480 Pharmaceutical transdermal compositions and method for treating inflammation in cattle Novel transdermal preparations combining a non-steroidal anti-inflammatory drug (NSAID) selected from groups such as oxicams (for example, meloxicam), propionic acids (for example, ketoprofen) and anthranilic acids (for example, tolfenamic acid), are disclosed. Methods for using and administering such preparation in the treatment of inflammatory conditions in bovines are also disclosed.
CN102988392A Application of Houttuynoid B to preparation of medicine for rising red blood cells The invention relates to a new application of a compound Houttuynoid B in the field of pharmacy, and particularly relates to an application of Houttuynoid B to preparation of a medicine for rising white blood cells, which is made public for the first time. As a framework type is brand-new, and the inhibitory activity of the Houttuynoid B to low red blood cells is unexpectedly strong, the possibility of obtaining any revelation from other compounds does not exist, and the Houttuynoid B has remarkable substantive distinguishing features and obviously has a notable progress to prevention and treatment of the low red blood cells.
EP1704139A1 DISUBSTITUTED CHALCONE OXIMES AS SELECTIVE AGONISTS OF RAR y RETINOID RECEPTORS Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RARϜ agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.
WO2011049659A3 Novel use and method of rapamycin to treat toxic shock Rapamycin is used for prevention and treatment of toxic shock. The toxic shock is induced, for example, by a toxin, such as Staphylococcal enterotoxin A (SEA), Staphylococcal enterotoxin B (SEB), toxic shock syndrome toxin 1 (TSST-I), streptococcal pyrogenic exotoxin A (SPEA), and streptococcal pyrogenic exotoxin C (SPEC).
US20090297536 Compositions, kits, and methods for identification, assessment, prevention and therapy of cancer The invention relates to compositions, kits, and methods for detecting, characterizing, preventing, and treating human cancer. A variety of chromosomal regions (MCRs) and markers corresponding thereto, are provided, wherein alterations in the copy number of one or more of the MCRs and/or alterations in the amount, structure, and/or activity of one or more of the markers is correlated with the presence of cancer.
CA2215066C Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
CN101538537B Pestalotiopsis fici, and discovery and application of Pestalotiopsis fici generated anti-tumor active compounds thereof The invention relates to a Pestalotiopsis fici N56 strain and discovery and application of generated anti-tumor active compounds thereof for preventing cervical carcinoma (HeLa) and colon cancer (HT29), belonging to the technical field of medicine. The solid fermentationis performed to the P.fici strain N56, the fermentation product is separated and purified to obtain active compounds Chloropupukeananin and PestalofoneC, and the structures of the active compounds are determined by using various technologies such as mass spectrum, nuclear magnetic resonance spectrum, and the like. The compounds have the remarkable antineoplastic activities after evaluation of the antineoplastic activity. The invention provides the alternative compound for studying and developing the new anti-tumor (cervical carcinoma and colon cancer) medicament and also provides the scientific basis for developing and utilizing the natural active material of the fungus source.
WO2009135433A1 Use of total salvianolic acid, panax notoginsenosides and combination thereof in treating septicemia The present invention provides new medical use of traditional Chinese medicines, especially use of total salvianolic acid, Panax notoginsenosides and combination thereof in treating and/or preventing septicemia.
US20110281808 Composition and Method for Increasing Pre Workout Thermogenics The present invention provides a composition for causing a simultaneous and synergistic increase in central nervous system activity and thermogenesis in a mammal, comprising Yerba Mate as a source of caffeine, hordenine and naringin. The present invention further provides a composition for causing a simultaneous and synergistic increase in central nervous system activity and thermogenesis in a mammal, comprising from 0.0001 g to 0.25 g of caffeine from Yerba Mate leaves, from 0.00001 g to 0.75 g of hordenine from barley and from 0.00001 g to 0.75 g of naringin sourced from grapefruit. The present invention finally provides a method for causing a simultaneous and synergistic increase in central nervous system activity and thermogenesis in an mammal prior to physical exercise, said method comprising providing a composition comprising a source of caffeine, hordenine and naringin and administering the composition to an mammal prior to physical exercise.
CN103610643A Preparation method of lipidosome applicable to water-soluble anthraquinone medicament The invention belongs to the technical field of medicines, and provides a water-soluble anthraquinone medicament applicable to large-scale industrial production and a preparation method thereof. A micronized water-soluble lipidosome support carrier is dispersed into an organic solvent or a supercritical fluid solvent into which a liposome membrane material is dissolved; the liposome membrane material is adsorbed on the micronized water-soluble lipidosome support carrier after solvent recycling is carried out under different pressure conditions, so as to obtain a micro-powder phospholipid-carrier compound; a proper hydration medium is selected to hydrate the phospholipid-carrier compound at proper temperature and pressure; the water-soluble carrier is quickly dissolved and lipid swells to form the liquid multi-layer lipidosome. According to the water-soluble anthraquinone medicament and the preparation method thereof, the phospholipid-carrier compound technology is adopted, and a proper ion medium is utilized, so that the water-soluble anthraquinone medicament is loaded by using the lipidosome, and thus the lipidosome which is uniform in particle size, stable in medicament loading capability and correlated characters is obtained.
US20100056484 Dietary supplemental composition effective for enhancing cognitive performance, elevating mood and reducing oxidative stress A dietary supplemental composition composed of Acetyl-L-Carnitine, Phosphatidylserine, L-Alpha-Glycerylphosphorylcholine, fish oils including Docosahexaenoic acid, Alpha Lipoic Acid, and optionally Eicosapentaenoic acid, and which in combination has been demonstrated to be effective in increasing cognitive performance, elevating mood and decreasing oxidative stress levels in mammals.
US20080279954 Drug delivery; therapeutic agent and crosslinked polymer network A method of preparing a supramolecular complex containing at least one therapeutic agent and a multi-dimensional polymer network is described. A supramolecular complex prepared by a method of the invention is described. A method of treatment by administering a therapeutically effective amount of a supramolecular complex of the invention is also described. Such a supramolecular complex may be used as a delivery vehicle for various therapeutic agents.
US7517858 Prodrugs of pharmaceuticals with improved bioavailability Lipid prodrugs of pharmaceutical agents and their analogs that have increased anticancer, anti-viral, anti-inflammatory, anti-proliferative activity over the parent drug, and methods for making lipid prodrugs. Compositions comprising lipid prodrugs for treating disease and methods for treating disease which involve using the compositions.
WO2007017643A1 3 , llB-CIS-DIHYDROTETRABENAZINE FOR THE TREATMENT OF A PROLIFERATIVE DISEASE OR AN INFLAMMATION The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a proliferative disease or an inflammatory disease, the compound being 3,1lb-cis-dihydrotetrabenazine or a pharmaceutically acceptable salt thereof.
EP1786418A1 Methods of treating proliferative skin diseases using carbazole derivatives The present invention relates to a method of treating a proliferative skin disease, comprising administering a therapeutically effective amount of a trk inhibitor.
US20090292008 Compositions and Methods for Treatment of Prostate and Other Cancers Therapeutic agents which target heat shock protein (hsp) 27 in vivo are used to provide treatment to individuals, particularly human individuals, suffering from prostate cancer and other cancers that overexpress hsp27. A therapeutic agent, for example an antisense oligonucleotide or RNAi nucleotide inhibitor with sequence specificity for hsp27 mRNA, for example human hsp27 mRNA, is administered to an individual suffering from prostate cancer or some other cancer expressing elevated levels of hsp27 in a therapeutically effective amount. The therapeutic agent is suitably formulated into a pharmaceutical composition which includes a pharmaceutically acceptable carrier, and packaged in dosage unit form. A preferred dosage unit form is an injectable dosage unit form.
US7597889 Recombinant polypeptides and nucleic acids; Graft-vs-host disease, host-vs-graft disease, organ transplant rejection, bone-marrow transplant rejection, autoimmune vasculitis, arthritis or asthma Disclosed are binding molecules which are recombinant polypeptides containing: (i) a binding domain capable of binding a target molecule, and (ii) an effector domain having an amino acid sequence substantially homologous to all or part of a constant domain of a human immunoglobulin heavy chain; characterized in that the binding molecule is capable of binding the target molecule without triggering significant complement dependent lysis, or cell mediated destruction of the target, and more preferably wherein the effector domain is capable of specifically binding FcRn and/or FcγRIIb. These are generally based on chimeric domains which are derived from two or more human immunoglobulin heavy chain CH2 domains domains. In preferred embodiments the regions 233-236, and 327-331, are modified, as are further residues to render the molecule null allotypic. Also disclosed are nucleic acids, host cells, production processes and materials, and uses. Pharmaceutical preparations are also disclosed.
EP1927378A1 Hair-treatment compositions comprising quercetin and use thereof to revitalize hair Hair-treatment material (I) containing at least one quercetin compound. An independent claim is included for a method for vitalising hair, reactivating the roots, activating the follicles, thickening the hair, promoting or enhancing hair growth, conditioning the hair and/or reducing and/or treating hair loss, by applying material (I) to the hair, the scalp or hairy skin, or to parts of the skin where hair growth has stopped but needs to be restarted.
CN103665071A Gopalamicin derivatives and application of same in inhibition of infection by drug-resistant bacteria and drug-resistant mycobacterium tuberculosis The invention relates to gopalamicin derivatives and application of the same in inhibition of infection by drug-resistant bacteria and drug-resistant mycobacterium tuberculosis. The derivatives are originated from fermentation products of marine actinomycete Streptomyces sp. 7-145. Results of experimental study show that discovered compounds with novel structures and known structures all have strong antibacterial activity on tested drug-resistant bacteria and drug-resistant mycobacterium tuberculosis and are expected to become clinically-useful novel drugs used for inhibition of infection by drug-resistant bacteria and drug-resistant mycobacterium tuberculosis.
WO2008117707A1 Ground crystal of olmesartan medoxomil Disclosed is an olmesartan medoxomil-containing preparation having a controlled dissolution rate. Specifically disclosed is an olmesartan medoxomil characterized by having a 90% particle diameter of not more than 75 μm. Also specifically disclosed is a method for producing an olmesartan medoxomil-containing preparation using the olmesartan medoxomil having such a particle diameter.
US20080275001 Enhanced bioavailability, absorption; using fartty acid, or salt thereof, or fatty ester; sustained release; drug is anticaogulant The invention relates to a solid oral dosage form comprising a pharmaceutically active ingredient in combination with an enhancer which enhances the bioavailability and/or the absorption of the active ingredient. Accordingly, a solid oral dosage form comprises a drug and an enhancer wherein the enhancer is a medium chain fatty acid ester, ether or salt or a derivative of a medium chain fatty acid, which is, preferably, solid at room temperature and which has a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is controlled release dosage form such as a delayed release dosage form.
CN1839846A Levofloxacin slow release micropill, its preparation method and uses The invention relates to a slow release micro-pellet preparation containing Levofloxacin, its preparation process and therapeutic use, wherein the micro-pellet preparation contains 0-40% of conventional medicinal particles and 60-100% of slow release medicinal micro-pellet, the micro-pellet contains medicinal core including Levofloxacin, and slow release coating layer whose content being 4-100% of the pellet core.
CN1813784A Compound medicinal formulation for treating acute-chronic vespiratory tract infection and its preparing method The present invention relates to a compound medicine preparation for curing acute and chronic respiratory tract infection. It is made up by using azithromycin and phlegm-removing active component according to the weight mixing ratio of 1:0.05-2.
US7919311 Compositions and methods for activating genes of interest Compositions and methods for activating genes of interest are provided. The compositions comprise a masked targeted expression cassette which expresses a gene product only in the presence of a target molecule. The cassettes are useful for the treatment of disease and for preventing the proliferation of neoplastic cells.
US20110046206 Double strand compositions comprising differentially modified strands for use in gene modulation The present invention provides double stranded compositions wherein the first strand is modified to have a particular motif and the second strand is modified a selected motif. The motifs are defined by positioning of differentially modified nucleosides wherein at least the sugar moieties are different. More particularly, the present compositions comprise an antisense strand that is modified to have a positional/full motif and the sense strand is modified to have an alternating motif, a hemimer motif, a blockmer motif, a gapped motif, a positional motif, a positional/full motif or a fully modified motif. Each strand further comprises one or more phosphorothioate internucleoside linkage. The compositions are useful for targeting selected nucleic acid molecules and modulating the expression of one or more genes. In preferred embodiments the compositions of the present invention hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. The present invention also provides methods for modulating gene expression.
CN103725649A Vegetable oil gel containing bFGF The invention provides a vegetable oil containing bFGF. The vegetable oil is formed by the following steps: linking the nucleotide sequence of the human bFGF to a 3' terminal of the nucleotide sequence of the oil protein of the oil expression plasmid p1390ONE to obtain the recombinant plasmid; transforming oil crops with the recombinant plasmid to express bFGF, and extracting the oil of seeds of the oil crops. The invention also provides a vegetable oil gel containing bFGF. The vegetable oil gel is formed by mixing the vegetable oil containing bFGF with a gel matrix of the oil, wherein the gel matrix comprises the following components in percentage by weight: 1-5% of carboxyethyl cellulose, 5-40% of glycerol, 0.01-0.1% of methylparaben, 0.01-0.1% of propylparaben and the balance of injection water. The vegetable oil gel containing bFGF comprises 30% of the vegetable oil containing bFGF and 70% of the gel matrix. The vegetable oil gel can be stored at 37 DEG C for 12 months, has no mould phenomenon and also has no change in physicochemical indices such as appearance and pH value. The vegetable oil gel can be stored at 4 DEG C for 12 months, and the activity of bFGF is not obviously changed.
WO2006128562A1 Use of chromone derivatives The invention provides for the use of chromone derivatives of the formula (I) or their physiologically unobjectionable salts, or a preparation comprising at least one compound of the formula (I) in which R 1, R2 and R3 are -H, -OH, -OA, -A, -OCOA R 1 and R2 together can be -methylenedioxy or -ethylenedioxy, R1, R2 and R3 are identical or different with the proviso that they cannot all together be -H, R4 is -H, -A, -COOH, -COOA, -COA, -CONH2, -CONHA X is -OH, -CH2-R4, -NH-R4 A is alkyl or R-substituted alky radical, benzyl or R-substituted benzyl radical, phenyl or R-substituted phenyl radical for the prophylaxis, improvement in general skin condition and/or treatment of skin diseases, especially hyperpigmentation, and also correspondingly new compounds.
CN101857861A Molecular marker for immunological recognition and construction and application thereof The invention relates to the field of immunology, in particular to a molecular marker for immunological recognition and construction and application thereof. The molecular marker for the immunological recognition has a turbot specific CpG-DNA sequence expressed by a base sequence in a sequence table SEQ ID. The base sequence in the sequence table SEQ ID can remarkably inhibit the invasion of pathogenic bacteria or be used as a vaccine adjuvant for enhancing the specificity of vaccines to inhibit the invasion of the pathogenic bacteria. Due to direct antibacterial capability and vaccine adjuvant effect, the obtained turbot specific CpG-DNA sequence has good application prospect in prevention and control of turbot diseases.
EP1861356A1 Imines as ion channel modulators The present invention provides a class of chemical compounds useful in the treatment of sickle cell disease, diseases characterized by unwanted or abnormal cell proliferation and for the treatment of ocular disorders such as glaucoma. The active compounds are tri-(aryl or heteroaryl) methane compounds or analogues thereof which further comprise an imine moiety and where the tertiary carbon atom can be replaced with a different atom such as Si, Ge, N or P. The compounds enhance resistance to degradation in a biological medium, inhibit potassium flux in a cell, reduce mammalian cell proliferation, reduce the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.
WO2013030150A1 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepines The invention relates to 6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepines, in particular for therapeutic purposes, to pharmaceutical agents, and to the use thereof in treatment, in particular for the prophylaxis and treatment of tumor diseases.
WO2008099368A1 Macrolide derivatives as antibacterial agents The present invention provides macrolide derivatives, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxella spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.
DE102004055284A1 Pharmaceutical composition containing phospholipid, sterol and negative charge carrier, useful in human or veterinary medicine for treating e.g. arthropod, protozoal and bacterial infections or tumors Pharmaceutical composition (A) comprises (a) a phospholipid (A1); (b) cholesterol, 7-beta -hydroxycholesterol and/or a beta -sitosterol (A2); and (c) a negative charge carrier (A3). Pharmaceutical composition (A) comprises (a) a phospholipid (A1) of formulae (I)-(VII); (b) cholesterol, 7-beta -hydroxycholesterol and/or a beta -sitosterol (A2); and (c) a negative charge carrier (A3), i.e. a 16-36C carboxylic acid, preferably saturated or (poly)unsaturated, especially with cis-double bonds; a bile acid; an amide of an amino acid with a fatty acid (saturated or (poly)unsaturated) or compound (VIII) R1>O-PO2->-O-(CH2)n-N+>R2>R3>R4> (I) R1>O-CH2-CH2-OP (III) R1>O-CH2-CH(OP)-(CH2)x-Me (IV) R2>1>OCH2-CH(OR2>2>)-CH2-OP (V) R3>1>O-CH2-C[((CH2)z-H)(CH2)y-H]-CH2-OP (VI) R4>1>-O-CH2-C(OH)(Me)-CH2-OP (VII) R5>1>-CONH-CH2CH2-O-PO2->-O-C H2CH(OH)-CH2OH Na+> (VIII) [Structure (II), page 37] R1>optionally saturated 15-26C hydrocarbyl; R2>, R3> and R4> each : hydrogen, 1-6C alkyl, 3-6C cycloalkyl or 2-5C alkylene, or two of them together form 2-5C alkylene; n : 2-6; R1>1>, R2>1>, R3>1> and R4>1>15-26C hydrocarbyl, saturated or (poly)unsaturated; R1>2> and R1>3>hydrogen, 1-6C alkyl or 2-6C hydroxyalkyl; m : 1 or 2; P : -PO2->-O-(CH2)n-N+>R2>R3>R4> or the residue of (II) after removing R1>1>O-; x : 0-4; R2>2>1-6C alkyl; y and z : 0-3, but not both 0; R5>1>15-25C hydrocarbyl; proviso: in (V) residues R2>1>, R2>2> and P can be distributed as wished over the positions in the glycerol molecule Independent claims are also included for the following: (1) use of erufosin (not identified) to prepare a composition for treating tumors; (2) (VII) as new compounds; and (3) method for preparing alkylphosphocholine compounds using plant oil, particularly olive oil, as starting material. - ACTIVITY : Acaricide; Cytostatic; Protozoacide; Antibacterial; Ophthalmological; Fungicide. No details of tests for any of these activities are given. - MECHANISM OF ACTION : Stimulation of leucopoiesis.
CN1899265A Medical dust cloud agent or granular agent and its use The medical atomized agent consists of chitin derivative and macromolecular isolator in the weight ratio of 100 to 0.1-99.9; or consists of chitin derivative and anti-phlogistic anodyne or spasm inhibitor in the weight ratio of 100 to 0.001-10. The medical atomized agent is used in surgical operation for preventing tissue adhesion and relieving pain and in clinical treatment for promoting wound healing and relieving pain.
CN102370629A Entecavir liquid capsule and preparation method thereof The invention relates to a medicinal preparation for treating hepatitis B, and especially relates to an entecavir liquid capsule and a preparation method thereof. Content of the entecavir liquid capsule comprises an entecavir raw material and accessories; the content is packaged in a hard capsule casing, and includes 0.02-2.0wt% of entecavir and 98-99.98wt% of accessories. The entecavir liquid capsule of the invention solves a homogeneity problem of main drug content in an entecavir low dosage preparation, and a problem of demanded simultaneous operations of copying, rubber processing and content wrapping of an existing soft capsule preparation technology, and problems of high moisture and high oxygen transmissivity, disadvantage for medicine storage and susceptibility to dehydration and ageing of the soft capsule, and difficulty in disintegrating and dissolving of a final product. Provided is an entecavir liquid capsule with good homogeneity, simple preparing process, high dissolution and high bioavailability.
CN102727495A Novel use of sanguinarine chloride The invention relates to a novel use of sanguinarine chloride and especially relates to a use of sanguinarine chloride in preparation of a drug for treating a thyroid cancer. In-vivo and in-vitro thyroid cancer experiments prove that sanguinarine chloride has effects of inhibiting or killing thyroid cancer cells, has human papilloma thyroid cancer cells IHH-4 and human anaplastic thyroid cancer cells ASH-3 growth IC50 values of 1.44 micromoles per liter and 2.62 micromoles per liter, and reduces a survival rate of thyroid cancer cells to less than 10%. A nude-mice in-vivo anti-cancer experiment proves that sanguinarine chloride has a transplantation tumor inhibition ratio of 80.81%.
US7138424 Indole derivatives, method for preparing same and pharmaceutical compositions containing same The present invention provides compounds of formula: and also provides their preparation and the pharmaceutical compositions comprising them. These compounds are ligands of CB2 cannabinoid receptors.
US20120046368 Method for purifying 3,4-dihydroxyphenylglycol (dhpg) from plant products Process for purifying 3,4-dihydroxyphenylglycol (DHPG) from any part of the plant, from the products or by-products derived from olive trees or any other vegetable product of the families Oleaceae, Orobanchaceae, Plantaginaceae, Compositae, Lamiaceae, Acanthaceae and/or Scrophulariaceae, and which comprises 1 or more steps wherein the initial product is introduced into at least one ion-exchange resin column, and in potentially subsequent steps the product eluted in the preceding column is introduced into an ion-exchange resin and/or a non-ionic adsorption resin column. Moreover, it relates to the DHPG extract obtainable by means of the process disclosed and to the applications thereof.
EP2586785A1 Phosphoric acid ester compound of hydroxy acid substituted phenyl ester, synthesis method and medical use thereof Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y = C1-4 straight carbon chain, M1 and/or M2 = H, alkali metal ion, protonated amine or protonated amino acid. The compound has good water solubility and high stability in its aqueous solution, and it can release 2, 6-diisopropylphenol rapidly under the action of enzymes in vivo, which has the effects of sedation, hypnosis and/or anesthesia. By protecting hydroxyl of 2, 6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2, 6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis and/or anesthesia.
CN1939895B Compound, composition and method for preventing from neurodegeneration in injury of central nervous system A composition for preventing nervous diseases accompanied with neuron death, its method and synthesis of BAS and its derivative are disclosed. BAS and its derivative prevent cortical neuron from beingdamaged by N-methyl-D-aspartate, zinc ion and active oxide cluster. It can be used to treat apoplexia, cerebral traumatism, spinal injury, epilepsy and other neurodegenerative diseases, which accompany with serious neuron lost.
US20110135674 Markers of XMRV Infection and Uses Thereof The present invention relates generally to assays for the detection of Xenotropic Murine Leukemia Virus-related Retrovirus (“XMRV”) and diseases associated with XMRV infection. Additionally, the invention relates to specific XMRV antigens capable of inducing an immunogenic response as well as XMRV-related nucleic acids having significant diagnostic, screening, and therapeutic utilities.
US20100168150 Camptothecin Analogue Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them. Compound of formula (I): wherein: R1, R2, R3, R4, R5, R80, R90, R81, R91, Alk, Alk′, X, X′ and G are as defined in the description. Medicinal products containing the same which are useful in the treatment of cancer diseases.
CN102871977A Ulipristal acetate dispersible tablet and preparation method thereof The invention relates to a ulipristal acetate preparation and a preparation method thereof, and particularly relates to a ulipristal acetate dispersible tablet with improved dissolution rate and a preparation method thereof. In order to solve the problem that the ulipristal acetate tablet in the prior art is low in dissolution rate and bioavailability and affects emergency contraception effects, the invention provides the ulipristal acetate dispersible tablet. The ulipristal acetate dispersible tablet is prepared from a premix compound of ulipristal acetate and a disintegrating agent and a excipient, wherein the content of ulipristal acetate is 1-30%(w/w) and accounts for 50-80% of the total weight of the premix compound, the particle sizes of 70-100% ulipristal acetate and the disintegrating agent are less than or equal to 75 micrometers. The ulipristal acetate dispersible tablet disclosed by the invention can take effect quickly in vivo, can realize more effective emergency contraception effect, and is wider in application range.
US20070270484 3'-N-Substituted-3-O-Substituted Erythronolide a Derivatives This invention generally relates to macrolides, more particularly, the invention relates to 3-N-substituted-3-O-substituted erythronolide A derivatives, which are antibacterial agents effective against gram positive or gram negative bacteria and atypical pathogens. The compounds of this invention are more particularly effective against Staphylococcus aureus, Streptococcus pneumoniae, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Haemophilus influenzae. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods for treating bacterial infection.
CN102327280A Medicinal composition for treating phimosis, and application thereof The invention discloses a medicinal composition for treating phimosis. The medicinal composition comprises a therapeutically effective amount of betamethasone or pharmaceutically acceptable salt thereof, a therapeutically effective amount of conjugated estrogens or pharmaceutically acceptable salt thereof and a therapeutically effective amount of anti-inflammatory medicine; and the medicinal composition is prepared into an external application preparation by using pharmaceutically acceptable auxiliary materials. When phimosis is treated by the composition, the composition has a treatment effect aiming at pathogenesis, is high in cure rate, and can relive the pain of a patient caused by phimosis. The medicinal composition is applied locally and is low in toxicity and is easy to withdraw timely.
US7655251 Amphiphilicmonocatenary glycosylated hydrocarbon nitrones; oxidation resistance;free radical scavengers; neuroprotectants; cosmetic products for the skin, hair andnails; imunotherapy; antiinflammatory agents; Alzheimer's disease; Parkinson'sdisease; aging resistance; radiation injuries Novel compounds, derivatives of α-C-phenyl N-tert-butyl nitrone, a method for production and use thereof for the preparation of medicaments for the prevention of treatment of diseases related to oxidative stress.
US7879966 pH-sensitive polymer A pH-sensitive polymer which has cytotoxic or membranolytic properties at pH values below pH 6.5. Carriers for natural or synthetic biomolecules or active pharmaceutical ingredients using such a pH-sensitive polymer.
WO2014077621A1 Composition for preventing hair loss and accelerating hair growth The present invention relates to a composition for preventing hair loss and accelerating hair growth represented by chemical formula 1, wherein A is derived from a polycyclic compound, and R is an alkyl oxy group or an acyloxy group comprising a carbon number of 1 to 20 and a saturated or an unsaturated straight chain or a branched chain.
CN101857619A Novel secoiridoid compound and application in preparation of anti-inflammatory drug The invention relates to a novel secoiridoid compound and application in the preparation of anti-inflammatory drugs. A novel compound is extracted and separated from gentiana straminea, has a chemical structural general formula shown in a formula I and has anti-inflammatory activity. The invention also relates to a use of the compound or pharmaceutically acceptable salts of the compound in the preparation of drugs, in particular to a use in the preparation of anti-inflammatory drugs. The invention also relates to a pharmaceutical composition taking the compound as a main component.
WO2011079291A1 Radiopharmaceutical complexes The invention provides compounds such as chelating agents useful in chelating metal ions, particularly radionuclides, to provide metal ion complexes. The invention also provides methods of using the compounds and complexes of the invention, such as in therapeutic and diagnostic applications.
US20100099648 Natural equivalent of chemically modified starch The present invention relates to a composition comprising citrus fruit fiber having a water binding capacity of from 8 to 25 (w/w) and native starch selected from the group consisting of corn starch, rice flour, sorghum starch, tapioca starch and mixture thereof.
EP2398792A1 Tosylate salt of a 5-pyrazolyl-2-pyridone derivative, useful in the treatment of copd 6-Methyl-5-(I -methyl-1H-pyrazol-5-yl)-N-{ [5-(methylsulfonyl)pyridin-2-yl]methyl }-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a form, and the use of such a salt and form in therapy.
CN101554365A Norfloxacin transdermal agent for preventing and curing yellow and white scour piglet and preparation method thereof The invention relates to a norfloxacin transdermal agent for preventing and curing yellow and white scour piglet, which is characterized by comprising the following medicaments by weight portion: 1 to 3 portions of norfloxacin and 1 to 2 portions of water-soluble azone with weight portion. The invention has the advantage of providing the norfloxacin transdermal agent for the piglets to prevent and cure yellow and white scour of the piglets. The invention has simple preparation method, obvious healing effect, simple and convenient use and wide application scope, not only avoids stress brought by sequentially catching the piglets, but also saves time and manpower, and reduces the labor intensity.
WO2008046573A1 Substituted sulfonamide derivatives for use as bradykinin 1 receptor modulators The present invention relates to substituted sulfonamide derivatives of general formula (I), to methods for the production thereof, pharmaceuticals comprising these compounds, and to the use of substituted sulfonamide derivatives for the production of pharmaceuticals for treating pain, especially acute, visceral neuropathic or chronic pain and inflammatory pain, such as migraine, diabetes, respiratory diseases, inflammatory intestinal diseases, neurological diseases, skin inflammations, rheumatic diseases, septic shock, reperfusion syndrome, obesity and for use as angiogenesis inhibitor.
CN102526051A Eye ointment for treating fungal keratitis The invention discloses eye ointment for treating fungal keratitis. The eye ointment is a mixture containing terbinafine hydrochloride and atropine. The eye ointment solves the problems that the anti-fungal eye medicine lacks and the conventional anti-fungal eye drop is expensive and short in persistence time in eyes, has a poor anti-fungal curative effect and cannot relieve secondary iridocyclitis of the fungal keratitis and the like. The invention has the advantages that: the eye ointment has long persistence time in the eyes and an obvious anti-fungal curative effect, the effective rate reaches 98 percent, and the eye ointment has a treatment effect on the secondary iridocyclitis, obviously relieves the eye pain symptom of a patient and does not have obvious toxic or side effect; the preparation method is simple, and has the feasibility of industrialized production; and the eye ointment is expected to play an important role in treating the clinical fungal keratitis.
WO2014158916A1 Substituted naphthyridine and quinoline compounds as mao inhibitors The invention provides a chemical entity of Formula (I), wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive or motor impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non- human animal training protocols, and treating treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.
CN102406617A Tecovirimat dry suspension and preparation method thereof The invention discloses a tecovirimat dry suspension and a preparation method thereof. The tecovirimat dry suspension provided by the invention comprises the following components in parts by mass: 20 to 30 parts of monoclinic crystal micro-powder of tecovirimat monohydrate, 40 to 80 parts of filler, 5 to 10 parts of suspending aid, and 1 to 5 parts of wetting agent, wherein, in the monoclinic crystal micro-powder of tecovirimat monohydrate, the space group of a monoclinic system is C2/c, cell parameters are as follows: a is 28.724 (2), b is 10.533 (1), c is 12.902 (1) tenthmeter and beta is 112.18 (1) degrees, the cell volume V is 3614.7 (6) cubic tenthmeter, and the number Z of molecules in unit cell is 8. The dry suspension solid powder has good liquidity, can be quickly transformed into a uniform and stable suspension after being mixed with water, has less foam, low deposition speed and excellent redispersibility, and is convenient for administration of patients. Animal experimentsprove that: the preparation has long half-life period, high blood concentration and strong mousepox virus resisting activity.
US20090197914 Piperidine Derivatives, Their Process for Preparation, Their Use as Therapeutic Agents and Pharmaceutical Compositions Containing Them The present invention provides a compound of a formula (I) wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.
CN1958590A Derivative of oxazole p-camptothecin ester, preparation method and application This invention relates to a kind of oxazolecamptothecin ester derivatives, and the definitions of R1, R2 and R4 are shown in the invention. This invention also discloses the method for preparing the derivatives, the drug compositions containing the derivatives and their applications. The compounds shown in formula I have anti-tumor activity.
US20100087487 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
CN1957930A Application of honokiol in preparing sensitization agent for tumour chemotherapy An application of honokiol (C18H18O2) along with its pharmacologically acceptable excipient or carrier in preparing the sensitizer for the chemicotherapy of cancer is disclosed. Said sensitizer is almost non-toxic to the normal cells of human body.
CN102898408A Benzopyran compounds, preparation method and applications thereof The present invention relates to compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof, wherein various groups are defined in an instruction. The present invention further relates to a preparation method for the compounds, and applications of the compounds in preparation of antivirus drugs or antitumor drugs. The present invention further relates to antivirus drug compositions or antitumor drug compositions containing the compounds or the pharmaceutically acceptable salts, and pharmaceutically acceptable carriers, wherein the virus is hepatitis B virus or influenza virus, and the tumors are respectively tumors generated in esophagus, stomach, intestines, mouth, pharynx, larynx, lung, colon, breast, uterus, endometrium, ovarian, prostate, testis, bladder, kidney, liver, pancreas, bone, connective tissue, skin, brain or central nervous system, or thyroid cancer, leukemia, Hodgkin's disease, lymphoma, or myeloma.
CN1985927B Medicine composition for treating hepatic disease mainly The present invention belongs to the field of medicine technology, and is especially one kind of medicine composition for treating liver diseases and its preparation process. The medicine composition is prepared with wolfberry fruit 50- 1000 weight portions, angelica 50-1000 weight portions, and glycyrrhizic acid or its pharmaceutically acceptable salt 1-50 weight portions; or with wolfberry fruit polysaccharide 2.5-50 weight portions, angelica polysaccharide 1-20 weight portions, and glycyrrhizic acid or its pharmaceutically acceptable salt 1-50 weight portions. It may be prepared into any pharmaceutically acceptable forms, preferably orally taken preparation and injection. It is used mainly for treating various liver diseases, including viral hepatitis, medicinal liver injury, fatty liver, alcohol liver, etc.
WO2012142377A1 Bicyclic methyl amine derivatives as sphingosine-1 phosphate receptors modulators The present invention relates to novel bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1 -phosphate receptors.
CN102451241A Calculus-bovis-sativus-containing medicine for clearing heat and removing toxicity The invention discloses a calculus-bovis-sativus-containing medicine for clearing heat and removing toxicity. The medicine comprises the following components by weight: 3 to 8g of calculus bovis sativus, 80 to 350g of rhubarb, 100 to 235g of gypsum, and 70 to 300g of scutellaria. In the calculus-bovis-sativus-containing medicine for clearing heat and removing toxicity, calculus bovis is replaced by the calculus bovis sativus, and rhubarb, gypsum, scutellaria, and other components are supplemented in an appropriate proportion, so the medicine is low in cost and has good effects of clearing heat and removing toxicity.
US20120142590 Methods and Compounds Regulating the Erythroid Response to Iron Deficiency The present invention discloses the signaling pathway involved in erythroid repression by iron deficiency. Further disclosed is a non-toxic small-molecule compound which potently reverses the erythroid repression caused by iron deficiency. The present invention further encompasses novel compounds for inhibition of red cell production, useful, for example, in the treatment of polycythemia vera, a malignancy causing uncontrolled red cell production. These inhibitory compounds also promote megakaryocytic lineage commitment and may therefore be useful for augmentation of platelet production. The present invention further discloses isocitrate reversal of iron deprivation.
WO2010000401A1 Use of substituted pyridinone carboxylic acid derivates for producing pharmaceuticals for the treatment of dyslipidemia The invention relates to the use of substituted pyridinone carboxylic acid derivates and the physiologically acceptable salts thereof for the production of pharmaceuticals for treating dyslipidemia. The invention relates to the use of compound of formula (I), where the group R has the indicated meanings, and to the physiologically acceptable salts thereof for the production of a pharmaceutical for treating dyslipidemia.
US20130231297 Dietary supplement for improving visual performance An orally administered composition and method for improving visual performance using the composition is provided. The composition comprises a combination of astaxanthin, saffron, lutein, zeaxanthin and European black currant extract in amounts effective to reduce eye fatigue or enhance at least one of visual acuity, contrast acuity, glare relief and recovery, or high intensity blue light filtration.
CN102198082B Micelle loaded with Tacrolimus or pharmaceutical salts thereof, lyophilized preparation as well as preparation methods and applications The invention belongs to the technical field of pharmaceutical dosage forms and nano medicine preparation, and more particularly relates to a micelle loaded with Tacrolimus or pharmaceutical salts thereof, a lyophilized preparation as well as preparation methods and applications thereof. In order to achieve the clinical application of the micelle provided by the invention, the drug loading, the encapsulation rate and the stability of the preparation need to be ensured. The micelle is prepared from biodegradable polymer materials and Tacrolimus or pharmaceutical salts thereof in parts by weight: 1 part of Tacrolimus or pharmaceutical salts thereof and 1.5-99 parts of degradable polymer materials, wherein the degradable polymer materials are diblock polymer methoxy polyethylene glycol-polycaprolactone (the molecular weight ratio of MPEG to PCL is 0.5-2), and triblock polymer polycaprolactone-polyethylene glycol-polycaprolactone (the molecular weight ratio of PCL to PEG is 0.5-3). The micelle using Tacrolimus or pharmaceutical salts thereof or the lyophilized preparation of the micelle can be used in medicines for anti-rejection in liver transplantation, kidney transplantation, lung transplantation, corneal transplantation and other organ transplantations.
WO2009134347A2 Sulfoalkyl ether cyclodextrin compositions SAE-CD compositions are provided, along with methods of making and using the same. The SAE-CD composition comprises a sulfoalkyl ether cyclodextrin and less than 100 ppm of a phosphate, wherein the SAE-CD composition has an absorption of less than 0.5 A.U. due to a drug-degrading agent, as determined by UV/vis spectrophotometry at a wavelength of 245 nm to 270 nm for an aqueous solution containing 300 mg of the SAE-CD composition per mL of solution in a cell having a 1 cm path length.
CA2656393A1 Method of using substituted piperidines that increase p53 activity The present invention discloses a method of using compounds, which have HDM2 protein antagonist activity, to treat or prevent cancer, other diseases caused by abnormal cell proliferation, diseases associated with HDM2, or diseases caused by inadequate P53 activity.
US20110183927 Compositions Comprising Sugar-Cysteine Products The present invention provides compositions comprising sugar, cysteine, and/or sugar-cysteine products, methods of preparing the same, and/or using the same.
EP0738328B1 Composition containing nucleic acids, preparation and uses The present invention relates to compositions comprising at least one nucleic acid and one lipopolyamine, and their utilisation in gene therapy, particularly for the transfert in vivo of nucleic acids.
WO2006041158A1 Method for modifying the ambience, and spray liquid and sprayer used in the method A solution obtained by dissolving Ϝ-aminobutyric acid as the solute in a solvent is sprayed in a room.
WO2010131712A1 Therapeutic pharmaceutical agent for diseases associated with decrease in function of gne protein, food composition, and food additive Disclosed are a therapeutic pharmaceutical agent for diseases associated with the decrease in the function of GNE protein, a food composition, and a food additive. The therapeutic pharmaceutical agent is characterized by comprising a compound capable of increasing the quantity of N-acetylneuraminic acid in cells. Examples of the compound to be contained in the therapeutic pharmaceutical agent include N-acetylneuraminic acid, an intermediate produced downstream from N-acetylmannosamine in an N-acetylneuraminic acid biosynthesis pathway, an N-acetylneuraminic acid derivative, an N-acetylmannosamine derivative, an N-acetylneuraminic acid-containing compound, an N-acetylneuraminic acid derivative-containing compound, an N-acetylmannosamine-containing compound, an N-acetylmannosamine derivative-containing compound, an inhibitor of a degrading enzyme for N-acetylneuraminic acid, an inhibitor of a degrading enzyme for N-acetylmannosamine, an inhibitor of a degrading enzyme for the intermediate, and others.
CN102010347A Biphenyl compound serving as antitumor medicament and preparation method thereof The invention discloses a biphenyl compound serving as an antitumor medicament and a preparation method thereof. The biphenyl compound has antitumor activities in vitro and in vivo, has the effects of inducing apoptosis and inhibiting proliferation on colorectal cancer cell lines, lung cancer cell lines, liver cancer cell lines, breast cancer cell lines or pancreatic cancer cell lines in vitro and has the effects of inhibiting tumors on liver cancers and colorectal cancers in vivo. The biphenyl compound can be applied to preparation of the antitumor medicament. The preparation method of the biphenyl compound has the advantages of readily available raw materials, mild reaction conditions, easily operated reaction processes and cheap and readily available reagents.
EP2462138A1 Antiviral compounds and methods of making and using there of cross reference to related applications Compounds which exhibit antiviral activity, particularly against influenza virus,and methods of making and using there of are described herein. In one embodiment, the compounds are heterocyclic amides containing piperazine and isozazole rings and optionally substituted with one or more substituents. The compounds can be formulated with one or more pharmaceutically acceptable excipients to form compositions suitable for enteralor parenteral administration. The compounds are preferably used to treat or prevent Influenza Ainfections, such as H1N1, H2N2, H3N2, H5N1, H7N7, H1N2, H9N2, H7N2, H7N3, and H10N7.
US20110077215 DNA Methylation As A Target For Diagnosis And Treatment Of Chronic Lymphocytic Leukema (CLL) Global DNA methylation is a predictor of aggressive disease in patients with chronic lymphocytic leukemia. The higher the DNA methylation, the more likely a patient is going to require systemic therapy. Although there is a gradual decline in global DNA methylation with increasing age in normal individuals, the methylation index only decreases by approximately 0.03 per decade. A pilot study was performed in which patients with chronic lymphocytic leukemia were treated with low doses of DNA methylation inhibitors to evaluate if inhibition of DNA methylation can translate into a clinical benefit. Inhibition of DNA methylation was observed to lead to re-expression of tumor suppressors and normal cellular function. At low non-toxic doses of 0.05-0.09 mg per kilogram per day for three days every 28 days, some patients with chronic lymphocytic leukemia were observed to achieve a reduction in circulating leukemia cells. This was observed to correlate with a reduction in global DNA methylation and an alteration in methylation of core histones.
CN101065130A Use of phospholipids for wound healing The present invention provides a phospholipid and a pharmaceutical composition comprising a phospholipid for use in the treatment of a wound by inducing hyaluronic acid secretion; and a method of treating a wound comprising the application of a phospholipid thereto.
CN101229377A Coordinated use method of trinosin magnesium chloride and sodium chloride injecta The invention relates to a matching usage method of trinosin-sodium magnesium injection and sodium chloride injection. The invention aims at solving problems existing in background technology: the mixture of trinosin-sodium magnesium injection and sodium chloride injection is inapplicable for diabetes sufferers; after trinosin-sodium magnesium injection and sodium chloride injection are mixed, 5-hydroxymethyl furaldehyde is easily produced and incidence of toxic as well as side effect is easily increased. The technical proposal for solving the technological problem is the matching usage method of trinosin-sodium magnesium injection and sodium chloride injection, which is characterized in that: 1 to 2 trinosin-sodium chloride injection, each containing 100mg of trinosin and 32mg magnesium injection are dissolved in 200-500ml of NaCl injection with concentration of 0.9 percent, which is fully mixed and intravenously dripped. The invention can be utilized in the matching usage of trinosin-sodium magnesium injection and sodium chloride injection, and has remarkable advantages of adaptability for diabetes sufferers, avoiding the probability of generation of 5-hydroxymethyl furaldehyde and guaranteeing medicinal safety.
CN101810859A Medical composition containing aniline derivative The invention relates to a medical composition which contains 2-[4-(2,5-difluorophenyl) methoxy] phenoxy]-5-ethoxyaniline or pharmaceutically acceptable salts or esters or a mixture thereof, at least one cardiovascular and cerebrovascular medicine and a pharmaceutically acceptable carrier and also relates to a kit containing the active matters. The composition or the kit is used for preventing and delaying the progress or treating the following diseases or symptoms: hypertension, salt sensitivity hypertension, renal hypertension, essential hypertension, pregnancy induced hypertension, hypertension complications, diabetes, diabete complications, dyslipidemia, ischemic diseases, coronary diseases, angor pectoris, congestive heart-failures, arrhythmia, cerebral apoplexy, arteriosclerosis, cerebral infarctions, cardiovascular and cerebrovascular diseases, coronary artery diseases and sexual dysfunction. The invention can reduce the morbidity and/or the mortality of the cardiovascular and cerebrovascular diseases, reduce adverse reactions and improve the compliance of taking medicines of patents meanwhile.
EP1868594A1 Ganglionic blocking agents for the treatment of epithelial diseases Compositions, and methods of making and using a composition, containing a ganglionic blocking agent and water provide increased penetration of the ganglionic blocking agent into and through epithelial surfaces, such as skin and mucosal surfaces, provide increased release from formulations containing such ganglionic blocking agents, and provide increased antiviral effectiveness compared with compositions containing a ganglionic blocking agents and lacking water.
US20120136066 Glomerulonephritis Treatment A compound of formula (I) R-L-CO—X (I) (wherein R is a C10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO2, said hydrocarbon group comprising at least 4 non-conjugated double bonds; L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO; and X is an electron withdrawing group) or a salt thereof for use in the treatment of glomerulonephritis.
EP1202975B1 Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
EP2416769A1 Method for preparing molecular complexes between adapalene and cyclodextrins The invention relates to a method for preparing molecular complexes between Adapalene and cyclodextrins using the technology of dense fluids under pressure, especially that of CO2.
CN101062013A Hydrochloride doxycycline injection for animals and the preparing method The invention discloses a muriatic acid ploys collar element injection for animals and preparation technology, which is characterized by the following: allocating main medicine, adjunct and dissolvent; choosing the main medicine as muriatic acid ploys collar element; choosing the adjunct as anti-oxidant; choosing the dissolvent as metal chelating agent and dissolvent for injecting. This invention develops a new preparation for veterinary clinical medicine, which possesses wide spread and strong drug-effect.
EP2040724B1 Biotherapeutic compositions comprising probiotic escherichia coli and metronidazole and uses thereof Biotherapeutic compositions of a non-pathogenic bacterial strain such as M-17 and its substrains and an anaerobic bacterial antibiotic such as metronidazole, are disclosed. Further disclosed are uses of M-17 or its substrains and an anaerobic bacterial antibiotic for treating disorders caused by anaerobic bacteria, whereby such disorders include, for example, pouchitis, microbial infection, irritable bowel syndrome, inflammatory bowel disease, mucous colitis and diarrhea.
DE102004046012A1 New D-glucopyranosylphenyl-substituted cyclic compounds useful as sodium-dependent glucose cotransporter inhibitors for treating metabolic diseases, e.g. diabetes D-glucopyranosylphenyl-substituted cyclic compounds (I) are new. D-glucopyranosylphenyl-substituted cyclic compounds of formula (I) and their tautomers, stereoisomers and salts, other than 3-(3-beta -D-glucopyranosyl-4,5-dimethoxybenzyl)-4-(3,4-dimethoxybenzyl)-dihydr o-2(3H)-furanone (Ia), are new: Cy : a 5- or 6-membered saturated or monounsaturated ring containing 0-3 heteroatoms (N, O, S) in which 1-2 CH2 groups can be replaced by CO, S, SO or SO2 and C-bonded H atoms can be replaced by F; Z : O, CH2, CH, NR, CO, S, SO or SO2, where CH2 and CH are optionally substituted with Me or F; R1>e.g. H, halo, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-7C cycloalkyl, (3-7C)cycloalkyl(1-3C)alkyl, 5-7C cycloalkenyl, (5-7C)cycloalkenyl(1-3C)alkyl, 1-4C alkylcarbonyl, aroyl; R2>H, F, Cl, Br, OH, 1-4C (fluoro)alkyl, 1-4C alkoxy, CN or NO2; R1>+R2>3-5C alkylene, 3-5C alkenylene or butadienylene, optionally substituted with F or 1-2 of Cl, OH, 1-3C alkoxy and 1-3C alkyl, where 1-2 CH2 groups can be replaced by O, S, CO, SO, SO2 or NR and 1-2 CH groups can be replaced by N; R3>R1> (but not iodo) or Y; R4>H, F, Cl, CN, NO2, NH2, mono- or di(1-3C alkyl)amino, 1-3C alkylcarbonylamino, 1-3C alkyl, 1-3C alkoxy, COOH, 1-3C alkoxycarbonyl, fluoromethyl or fluoromethoxy; R3>+R4>2-6C alkylene or 4-6C alkenylene optionally substituted with F or 1-2 of Cl, OH, 1-3C alkoxy and 1-3C alkyl, where 1-2CH2 groups can be replaced by O, S, CO, SO, SO2 or NR; or R3>+R4> forms a fused 5- or 6-membered ring optionally substituted with F or 1-2 of Cl, OH, 1-3C alkoxy and 1-3C alkyl, where 1-2 CH2 groups can be replaced by O, S, CO, SO, SO2 or NR and 1-2 CH groups can be replaced by N or a fused aromatic ring can be substituted with 1-2 of L; R5>H, F, Cl, CN, 1-3C alkyl, 1-3C alkoxy, fluoromethyl or fluoromethoxy; R4>+R5>1-4C alkylene or 2-4C alkenylene, optionally substituted with F or 1-2 of Cl, OH, 1-3C alkoxy and 1-3C alkyl, where 1-2 CH2 groups can be replaced by O, S, CO, SO, SO2 or NR; R6>H, 1-3C alkyl or F; R4>+R5>+R6>3-6C alkanetriyl optionally substituted with F or 1-2 of Cl, OH, 1-3C alkoxy and 1-3C alkyl, where 1-2 CH2 groups can be replaced by O, S, CO, SO, SO2 or NR; Y : e.g. O, CH2 (optionally substituted with F, Cl, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-7C cycloalkyl, 5-7C cycloalkenyl or Y is =C(Ry)DBRb; D : CO or SO2; Ry : H, F, Cl, CN, CF3 or 1-3C alkyl; B : a bond, O or NR; Rb : e.g. H, 1-6C alkyl, 3-6C alkenyl, 3-6C alkynyl, 3-7C cycloalkyl, 5-7C cycloalkenyl, (3-7C)cycloalkyl(1-3C)alkyl; Rb+B : pyrrolidine, morpholine, piperidine, piperazine of 4-(1-4C alkyl)piperazine; R : H or 1-4C alkyl; L : halo, 1-3C alkyl, CHF2, CF3, 1-3C alkoxy, OCHF2, OCF3, CN; R7a, R7b, R7c, R7d : H, (1-18C alkyl)carbonyl, (1-18C alkoxy)carbonyl, arylcarbonyl or aryl(1-3C)alkylcarbonyl; aryl : phenyl or naphthyl substituted with 0-2 of L; heteroaryl : e.g. pyrrolyl, furyl, thienyl, imidazolyl or pyridyl. [Image] - ACTIVITY : Antidiabetic; Antilipemic; Antiarteriosclerotic; Anorectic; Hypotensive; Cardiant; Antiinflammatory; Antigout. - MECHANISM OF ACTION : Sodium-dependent glucose cotransporter (SGLT) inhibitor. Test details are described but no results given.
US20080221217 Phenyl Compounds and Their Use in the Treatment of Type II Diabetes The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (xx); X is selected from CH, CF and N, R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12, R9 is selected from H and —C(O)NR1OR11, R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
EP1874789A1 Fluorinated 3'-deoxythymidine derivatives, a method for their preparation and their use The invention relates to new side chain-fluorinated 3'-deoxythymidine derivatives of the general formula (I) or physiological acceptable esters thereof, wherein R = CH218F; CH18F2; CH2F or CHF2 and Y = H, N3 or Hal. The invention also relates to a simple and efficient method for the preparation of these 3'-deoxythymidines of formula (I) and to the use of the 18F-containing compounds of formula (I) or of a pharmaceutical composition comprising these compounds for the diagnosis of tumors in positron emission tomography (PET).
CN103054833A A formula of an antimicrobial oil emulsion microcapsule for veterinary use The invention discloses a formula of an antimicrobial oil emulsion microcapsule for veterinary use, wherein per 1000g of the antimicrobial oil emulsion microcapsule contains 50-100g of an antimicrobial agent, 250-500ml of oil for injection, 250-500ml of water for injection, 1-5g of PEG, 5-10ml of sorbitan fatty acid ester, 5-10ml of polyoxyethylene sorbitan fatty acid ester, 250-500g of soluble starch, and 50-100g of methyl cellulose. According to the present invention, the oil emulsion is developed to be microcapsules which can be used for oral administration, thereby maintaining the long-acting and sustained-release effects of the oil emulsion, while in a large extent preventing disadvantages and side reactions in the production and application of the oil emulsion. The preparation process of the microcapsules is relatively simple, reducing the use of organic solvents and thereby reducing the cost of the product.
EP2589381A1 Compositions for improving or preserving lung function in a patient with a pulmonary disorder The described invention provides a pharmaceutical compositions for use in treatment methods for improving or preserving lung function in a patient suffering from a pulmonary disorder comprising an inflammatory component, the pharmaceutical compositions comprising a therapeutically effective amount of N-acetylcysteine, a derivative of N-acetylcysteine, or a pharmaceutically acceptable salt of N-acetylcysteine, wherein the therapeutically effective amount is effective to improve or preserve the lung function in the patient.
CN101919834A Application of 4-[(3-([(2-naphthoxo)acetyl] hydrazono) n-butyryl)amine] benzamide (FD2) in preparing antitumor medicaments The invention discloses belongs to the fields of genetic engineering and chemistry, relating to application of 4-[(3-([(2-naphthoxo)acetyl] hydrazono) n-butyryl)amine] benzamide (FD2) in preparing antitumor medicaments. The invention provides the application of the small molecular compound 4-[(3-([(2-naphthoxo)acetyl] hydrazono) n-butyryl)amine] benzamide in preparing the antitumor medicaments. The compound can obviously inhibit the proliferation of tumor cells. FD2 is a medicament designed aiming at a cell target spot CYPJ (Cycliphilins-J) and has difficult drug resistance formation and particularly effect on tumor cells with high-expression CYPJ proteins. Therefore, the small molecular compound of the invention is developed as a new antitumor medicament with obvious tumor suppression effect and good specificity. Accordingly, the FD2 of the invention can be developed as the new antitumor medicament, therefore, the invention provides a new approach and means for treating and curing tumors.
EP1977643A1 Manufacture of a viable, storable worm egg suspension Orally administrable pharmaceutical composition production involves utilizing a storable suspension of viable of surviving eggs of parasitic, non human pathogen helminths of Trichuris suis. A sufficient number develops in helminth after taking the suspension, which is applied for stimulation of regulatory human T-cells. The suspension of the helminth eggs is treated in a sulfuric acid solution having a pH value less than 2. The pH value is adjusted more than 4 and a pharmacological acceptable preservative is added. An independent claim is also included for an orally administrable pharmaceutical composition, which has a storable suspension of parasitic, non humanpathogen helminths, where a sufficient number is developed in helminth after taking the suspension.
WO2008050836A1 Agent for ameliorating adverse side-effect of chemotherapeutic agent Chemotherapeutic agents cause the decrease in the number of erythroid progenitor cells, as their adverse side-effect. A chemotherapeutic agent comprising arginine as an active ingredient can ameliorate the adverse side-effect. Thus, provided is an agent for ameliorating an adverse side-effect of a chemotherapeutic agent.
CN102657624A High optical purity trans-dextro oxaliplatin lyophilized powder injection and preparation method thereof The invention relates to a high optical purity trans-dextro oxaliplatin lyophilized powder injection and a preparation method thereof. The lyophilized powder injection contains high optical purity trans-dextro oxaliplatin with treatment effective dose and pharmaceutically acceptable lyophilized excipient, and does not contain animal-based auxiliary lactose, wherein the optical purity of the trans-dextro oxaliplatin is not lower than 99.95 percent; the pharmaceutically acceptable lyophilized excipient is one or more of cane sugar, trehalose, glycine, histidine, dextran, polyethylene glycol andcyclodextrin. The preparation method of the lyophilized powder injection comprises the following steps: dissolving raw and auxiliary materials in water; subpackaging, pre-freezing, lyophylizing, performing analytic drying; infiltering nitrogen into subpackaged bottles after the lyophilization is completed; and pressing plugs and caps. The high optical purity trans-dextro oxaliplatin lyophilized powder injection is used for preparing an anti-cancer medicament, and can be applied in a parenteral way after being re-dissolved with a compatible solution.
US20050004093 Using 6-betahydroxymethylpenicillanic acid sulfone; bactericides; therapy for bacteria infections in mammals Prodrugs of 6-β-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, each X is methylene, and Y is O, or wherein R is H, each X is O and Y is methylene, and solvates thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention, or a solvate thereof, an optional beta-lactam antibiotic and at least one pharmaceutically acceptable carrier. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a beta-lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.
US20050113426 Polyhydroxylated benzene-containing compounds A method for reducing food intake in a subject and a method for reducing the levels of an endocrine in a subject. The methods include administering to the subject in need thereof an effective amount of a compound of the formula: Also disclosed is a liposomal preparation which includes a liposome and a compound entrapped therein. The entrapped compound is of the formula shown above.
WO2011062253A1 Novel fused pyrimidine derivative Disclosed is a prophylactic and/or therapeutic agent for diseases associated with autoimmunity, immune deficiency diseases or neurodegenerative diseases, said prophylactic and/or therapeutic agent containing a novel fused pyrimidine derivative. Particularly disclosed is a prophylactic and/or therapeutic agent for sepsis.
CN1583773A Preparing method for raffinose calcium and use for raffinose as calcium-supplementing agent Calcium gossypose as an effective calcium supplement tonic is produced by: dissolving edible gossypose in water, adding calcium; stirring reaction at 2 - 10 deg.C; Filtrating to get cakes then drying them to obtain the reactant A; heating the filtration solution to 70 -96 deg.C, filtering to get cakes and drying them to obtain reactant B; finally, mixing A with B to obtain calcium gossypose product. The product comprises calcium gossypose, sweetener, fragrant agents, carrier materials and appropriate water. It is better than calcium carbnate, especially good for babies and youths.
WO2008126782A1 Antiseptic agent for skin Disclosed is a skin antiseptic agent which hardly causes a skin disorder such as rough skin and has a prolonged antiseptic effect. Also disclosed is a skin disinfection method which hardly causes a skin disorder such as rough skin and enables a prolonged antiseptic effect. The skin antiseptic agent comprises an N-acylated form of hydroxyproline or a salt thereof. A preferred example of the N-acylated form of hydroxyproline or the salt thereof is N-acetylhydroxyproline. Preferred examples of the antiseptic component include alcohols such as ethanol and isopropyl alcohol. The skin disinfection method may comprise applying or spraying a composition comprising an N-acylated form of hydroxyproline or a salt thereof onto the skin. The composition is preferably the skin antiseptic agent.
CN103330944A Bicyclol oral solid pharmaceutical composition, and preparation and preparation method thereof The invention relates to a bicyclol oral solid pharmaceutical composition which comprises an active component bicyclol and a medicinal adjuvant, wherein the medicinal adjuvant comprises a solubilizer and a filler, the solubilizer accounts for 0.2-5 times by weight of the bicyclol, and the filler accounts for 3-50 times by weight of the bicyclol. The invention also relates to an oral solid preparation prepared from the pharmaceutical composition and a preparation method thereof. The oral solid preparation provided by the invention has higher bioavailability than the common bicyclol tablets in the market, has the advantages of high disintegration speed, high dissolution, simple preparation technique and cheap and accessible adjuvant, and can easily implement industrial production.
US20090082360 Use of tyrosine kinase inhibitors for treating CNS disorders The present invention relates to a method for treating CNS disorders, more particularly selected from the group consisting of depression, schizophrenia, anxiety, migraine, memory loss, pain and neurodegenerative diseases, comprising administering a compound capable of depleting mast cells to a human in need of such treatment. Such compounds can be chosen from tyrosine kinase inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.
WO2010119102A3 Pharmaceutical composition containing proton pump inhibitor for treating dermatological autoimmune diseases The invention relates to a pharmaceutical composition for treating dermatological autoimmune diseases, comprising a proton pump inhibitor.
CN101584716A Red yeast rice extract oil and the preparation and application of the soft capsule thereof Disclosed is a red yeast rice extract oil and the preparation and application of the soft capsule thereof. The preparation method comprises: adding solvent into the red yeast rice medicinal material, heating for backflow for 2-5 hours; filtering, adding the filter residue into the solvent, heating for backflow for 1-4 hours; merging the filtrates; condensing at 50-90 degrees centigrade into extract with relative density of 1.1-1.4 at 25 degrees centigrade; adding ethanol by amount of 1-4 times (mass) of the red yeast rice medicinal material into the extract; dissolving, filtering, recovering ethanol to obtain stiff paste; adding ethanol by amount of 0.5-1 times (mass) of the red yeast rice medicinal material into the stiff paste; distilling to dryness at 60-95 degrees centigrade, insulating thermal for 1-5 hours; adding 0.5-4 times of ethanol into the extract; adding 0.5-5 times of vegetable oil, stirring uniformly at 50-70 degrees centigrade; recovering the ethanol to obtain the red yeast rice extract oil. The content of the active ingredient: lovastatin in the soft capsule prepared by the red yeast rice extract oil is 0.2-1.2wt%; the soft capsule is applied for preparing medicament for treating hyperlipemia; The invention can remove the large amount of unavailability components in the red yeast rice, and increases the content of lovastatin compounds in the extract of per weight unit effectively.
EP1026246B1 Avian infectious herpesvirus recombinants and recombinant vaccines prepared with the use of the same Turkey herpesvirus (HVT) recombinants or Marek's disease virus (MDV) recombinants contructed by integrating a heterogenous gene, in particular, a heteroantigen gene into the non-essential region of the HVT genome or the MDV genome, thus providing HVT recombinants carrying a foreign gene inserted into the gene region which is the untranslated region of the HVT genome; and vaccines containing these HVT recombinants.
US20120264803 Method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients The present invention provides a method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients who have been treated with transarterial embolization and an antitumor agent for treating cancer patients who have been predicted to have a high probability of obtaining sufficient therapeutic effects from such chemotherapy. The present invention also provides a method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients who have been treated with transarterial embolization using the expression level of PDGF-BB or IL-8 as an indicator and an antitumor agent for treating cancer patients who have been predicted to have a high probability of obtaining therapeutic effects by such prediction method.
EP1280566B1 Growth factor modified protein matrices for tissue engineering Proteins are incorporated into protein or polysaccharide matrices for use in tissue repair, regeneration and/or remodeling and/or drug delivery. The proteins can be incorporated so that they are released by degradation of the matrix, by enzymatic action and/or diffusion. As demonstrated by the examples, one method is to bind heparin to the matrix by either covalent or non-covalent methods, to form a heparin-matrix. The heparin then non-covalently binds heparin-binding growth factors to the protein matrix. Alternatively, a fusion protein can be constructed which contains a crosslinking region such as a factor XIIIa substrate and the native protein sequence. Incorporation of degradable linkages between the matrix and the bioactive factors can be particularly useful when long-term drug delivery is desired, for example in the case of nerve regeneration, where it is desirable to vary the rate of drug release spatially as a function of regeneration, e.g. rapidly near the living tissue interface and more slowly farther into the injury zone. Additional benefits include the lower total drug dose within the delivery system, and spatial regulation of release which permits a greater percentage of the drug to be released at the time of greatest cellular activity.
US7169772 Vasopressin active material; antidiabetic agents; diuretics; bioavailability 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivatives, which have excellent arginine vasopressin V2 activity and are useful for a drug for the treatment of central diabetes insipidus and/or nocturia.
DE102006037632A1 Microbiological mixture, useful for applying on a skin surface to treat e.g. fungus and bacteria infections, comprises piezoelectric nano-structures, reductive/oxidative microorganisms, conjugated biopolymer and/or 5-aminolevulinic acid Microbiological mixture (I) for applying on a skin surface, comprises piezoelectric nano-structures, reductive/oxidative microorganisms, at least one conjugated biopolymer and/or 5-aminolevulinic acid. Independent claims are included for: (1) a method for applying (I) on a skin surface, comprising applying (I) on the skin surface; drying the mixture; and removing the mixture from the skin surface; and (2) an arrangement for the execution of a procedure for applying (I) on the skin surface. - ACTIVITY : Fungicide; Antibacterial; Dermatological; Vulnerary; Virucide; Antiseborrheic; Antiinflammatory; Antipruritic; Antipsoriatic. - MECHANISM OF ACTION : None given.
US20090233953 Antagonists of the vanilloid receptor subtype 1 (vr1) and uses thereof The present invention is directed to compounds of formula (I) wherein variables X1, X2, Y, R1a, R1b, R2a, R2, A1, A2, A3, and A4 are as defined in the description, and methods of use to treat pain, neuropathic pain, allodynia, pain associated with inflammation or an inflammatory disease, inflammatory hyperalgesia, bladder overactivity, and urinary incontinence.
US6995186 For therapy of allergic or inflammatory disorders of the eye and nose Topical formulations of olopatadine for treatment of allergic or inflammatory disorders of the eye and nose are disclosed. The aqueous formulations contain approximately 0.17-0.62% (w/v) of olopatadine and an amount of polyvinylpyrrolidone or polystyrene sulfonic acid sufficient to enhance the physical stability of the formulations.
CN102600150A Application of paroxetine compound in preparing information treatment drug, preparation method and prepared novel drug The invention discloses application of a paroxetine compound in preparing an information treatment drug, a preparation method of the paroxetine compound and a novel drug prepared by the preparation method. During the treatment, the information treatment drug does not directly touch a human body, drug substance components are not consumed, chemotherapy effects can be achieved only by utilizing drug information physiotherapy, and the therapy window is enlarged more than one thousand times, and side effects of the chemotherapy are avoided. After paroxetine is used as the information treatment drug, the effective component content is not changed, and paroxetine can be used secondarily and effectively as a chemotherapy normal preparation.
WO2012089180A1 Form c of prasugrel hydrobromide and a method for its production A polymorphous form of the hydrobromide of prasugrel, a well-known substance reducing blood coagulation, prasugrel of formula (I), which is characterized by high chemical stability, and a method for its production. (Formula (I))
US8048451 Microparticles for use in a pharmaceutical composition for pulmonary administration, each microparticle comprising a particle of an active substance having, on its surface, particles of a hydrophobic material suitable for delaying the The invention provides microparticles for use in a pharmaceutical composition for pulmonary administration, each microparticle comprising a particle of an active substance having, on its surface, particles of a hydrophobic material suitable for delaying the dissolution of the active substance. The invention also provides a method for making the microparticles.
US20110280945 Novel method for the preparation of granulates of active constituents, and granulates as obtained The present invention relates to a method for preparing a granulate of at least two active principles, including a step of applying said active principles to a solid particulate medium by dusting, said active principles not being plant extracts.
CN102727894A Pharmaceutical composition for treating diabetes and its complications and application thereof The invention discloses a pharmaceutical composition for treating or preventing diabetes or its complications and an application thereof, and belongs to the medical field. According to the pharmaceutical composition, an insulin sensitizer and bromocriptine or its medicinal salt are used as active pharmaceutical ingredients. When the pharmaceutical composition is used to treat or prevent diabetes or its complications, the medical action modes are complementary. Therefore, the pharmaceutical composition shows remarkable synergism in the hypoglycemic aspect, has low adverse reaction, requires a low price and has a good application prospect.
EP1414457B1 Chiral dinapsoline The present invention relates to the preparation of the optical isomer (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de]isoquinoline. This invention also relates to the use of pharmaceutical compositions comprising (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de]isoquinoline for use for the treatment of movement disorders.
US20100120743 11Beta-Hydroxysteroid Dehydrogenase Type 1 Active Compounds A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
WO2009012679A1 2,2,3a,4-TETRAHYDROTHIOCHROMENE[4,3-C]PYRAZOLE COMPOUNDS, PREPARATION METHOD AND USAGE THEREOF The invention discloses 2,2,3a,4-tetrahydrothiochromene[4,3-c]pyrazole compounds of formula (I) or (II) and their stereoisomers, racemic mixtures or nonracemic mixtures of the stereoisomers, or pharmaceutically acceptable salts or solvates. The invention also discloses their preparation method, pharmaceutical compositions and the antifungal use.
CN102079759A 6-substituted quinazoline derivative, preparation method and application thereof The invention belongs to the technical field of pharmaceutical chemistry and discloses quinazoline derivatives as shown in a general formula (I), wherein the R1 and R2 are defined by the specification. The invention also discloses a preparation method for the derivatives, physiologically acceptable salts formed by the derivatives and inorganic or organic acid or alkali as well as a pharmaceutical composition containing the derivatives and the physiologically acceptable salts. The compounds have the valuable pharmacological properties, especially the inhibitory effect on the signal transduction caused by tyrosine kinase. The invention also discloses a method for treating diseases, especially treating diseases which have the characteristic of abnormal erbB family protein tyrosine kinase (PTK) activity.
EP1259474B1 Calcium dicarboxylate ethers, methods of making same Alcohol and water solvates of 6-(5-carboxy-5-methyl-hexyloxy)-2,2-dimethylhexanoic acid monocalcium salt are crystalline and have the formula (I), wherein R1 is H or lower alkyl, and x is a number from 0 to 10, and are useful for treating dyslipidemia.
US20130065909 Fatty acid fumarate derivatives and their uses The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.
CN1837202A Flavonols with blood-fat-lowering effect The invention discloses a flavonol compound with general formula I structure in the medical health domain, which is characterized by the following: the structure is showed on the picture, the flavonol kind compound is get by condensating and ringing replacement ortho-hydroxyethanone and replacement benzaldehyde; the compound can be used for reducing serum triglyceride, reducing LDL cholesterol level and improving HDL cholesterol level, which can treat hyperlipemia and prevent peripheral angiopathy, coronary disease, atherosclerosis, angiostenosis and have application in cardiovascular disease drug.
CN103202832A Application of acylated tanshinol derivant in prevention and treatment of cardiovascular disease and complication thereof The invention discloses application of a compound shown in a structural general formula (I) in the specification in prevention and treatment of a cardiovascular disease and complication thereof, wherein R1, R2 and R3 are independently selected from hydrogen, benzoyl or C2-C6 acyl, but not H at the same time; and M is H<+>, Na<+> or K<+>. Tanshinol is taken as a material; and a plurality of acylated tanshinol derivants are prepared by acylation reaction. Therefore, not only is easily oxidized hydroxyl protected, but also the lipid solubility and the transmembrane transport capacity are also increased; and an experiment proves that acylated tanshinol has significant protection effect on rat myocardium with ischemia reperfusion injury.
US20110046042 Long Interspersed Nuclear Element Polypeptide Compositions and Methods of Use Thereof The present invention provides LINE polypeptides; and compositions, including immunogenic compositions, comprising a subject LINE polypeptide. The present invention provides a recombinant nucleic acid comprising a nucleotide sequence encoding a subject LINE polypeptide. A subject composition is useful for stimulating a T-cell immune response to a LINE peptide. The present invention further provides methods of stimulating an immune response in an individual to a retrovirus- or lentivirus-infected cell. The present invention further provides methods of treating cancers that are associated with tissues in which LINE polypeptides are aberrantly expressed. Also provided are methods of treating disorders, involving decreasing an immune response to a LINE polypeptide.
US7169753 Such as magnesium-containing tetrahydroporphyrin for use in photodynamic therapy, tumor diagnosis, bactericides, and viricides; transesterification Novel C-132-COXR1, C-172-COXR2 and C-132-COXR1, C-172-COXR1 derivatives of chlorophyll and bacteriochlorophyll compounds are provided wherein X is O, S or N and R1 and R2, the same or different, may be an optionally substituted hydrocarbyl, amino acid, peptide, protein or saccharide radical. The compounds are for use in photodynamic therapy (PDT), for diagnosis of tumors, and for killing cells and infectious agents such as bacteria and virus, both in biological products and in living tissues.
WO2008028410A1 Use of low molecular weight fucoidan in the preparation of medicament for the treatment of cardiovascular and cerebrovascular diseases Use of low molecular weight fucoidan in the preparation of medicaments for the treatment of cardiovascular and cerebrovascular diseases, especially for the treatment of ischemic cardiovascular and cerebrovascular diseases, wherein the ischemic cardiovascular and cerebrovascular diseases contain coronary heart disease having no symptom, angina, cardiac infarction, arrhythmia, cerebral hemorrhage and cerebral infarction, etc. The low molecular weight fucoidan of the invention can be degraded from the fucoidan extracted from kelp, fucus vesiculosus, ascophyllum nodosum, ecklonia kurome or chorda filum, etc, and the preferred low molecular weight fucoidan of the invention can be degraded from the fucoidan extracted from kelp and its molecular weight is 8000~10000.
CN102861016A Application of jatrorrhizine for treating candida albicans infectious diseases The invention discloses a novel application of jatrorrhizine for treating candida albicans infectious diseases. The jatrorrhizine can be extracted from plants of coptis roots, amur corktree barks, caulis mahoniae and the like. The study shows that half bacteriostasis concentration of the jatrorrhizine to candida albicans is 139+/-21mg/L, and effective dose of the jatrorrhizine for enhancing body resistibility of a low immune function mouse to the candida albicans is 30mg/Kg. The jatrorrhizine and pharmaceutically acceptable salts, esters or sugars, excipients and the like are utilized for preparing medicines for treating diseases caused by the fact that the candida albicans infect human and livestock, and the jatrorrhizine can be applied to, but is not limited to, medicines for treating human skins, mucous membranes, internal organs or nervous centralis candidiasis, livestock upper digestive tract mycoses and the like. The jatrorrhizine and the pharmaceutically acceptable salts, esters or sugars and excipients and the like can be prepared to be injection, oral administration and external preparations and dosage forms thereof which are pharmaceutically acceptable such as injections, tablets, capsules, liniments, pastes, smearing agents, emulsions, nanoparticle emulsions, and the like.
WO2009103199A1 A g-csf conjugate modified by water-soluble polymer Provided are a G-CSF conjugate modified by water-soluble polymer having the formula: water-soluble polymer-linking group-N-terminal-G' or pharmaceutically acceptable salts thereof, the preparation method thereof and the pharmaceutical composition comprising the same.
US20090048185 Therapeutic Drug for Suppressing Functions of NKT Cells Containing Glycolipid Derivative as Active Ingredient A therapeutic drug for diseases, in which NKT cells or stimulus of NKT cells is involved in deterioration of disease conditions, containing, as an active ingredient, a glycolipid derivative having the formula (I): wherein R1 indicates an aldopyranose residue, R2 indicates a hydrogen atom or a hydroxy group, A indicates —CH2—, —CH(OH)—CH2— or —CH═CHCH2—, x indicates an integer of 13 to 16 and y indicates an integer of 0 to 25 or its pharmacologically acceptable hydrate or solvate.
US20120178671 Inhibition of nfk-b mediated virus replication with specific oligosaccharides The inventors surprisingly found that specific oligosaccharides are capable of inhibiting viral replication through inhibiting NF-κB activation. The invention thus pertains to a composition comprising pectin (in the form of digalacturonic acid, trigalacturonic acid, polygalacturonic acid), Arabinoxylan from rice bran, β-glucan from bakers yeast, D-Ribose or mixtures there-of for inhibiting viral replication in a mammal with a viral disease.
CA2372912C Method of using cyclooxygenase-2 inhibitors in the treatment and prevention of neoplasia This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically--effective amount of a compound of Formula I. (see formula I) wherein A, R2 and R3 are as described in the specification.
US20080051441 Aryl Sulphonamide Modulators Compounds of Formula I: wherein R1, R2, R3, R4, R5 Ar1 and X are as described in the specification, pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission.
CN103127059A Oral administration preparation composed of bilobalide B derivative and preparation method thereof The invention discloses an oral administration preparation composed of a bilobalide B derivative and a dry granulating method thereof. According to the oral administration preparation composed of the bilobalide B derivative, every 1000 pieces of preparations contain 50g of bilobalide B derivatives, and then the oral administration preparation (such as a tablet, a capsule, and a granule) is produced. According to the oral administration preparation composed of the bilobalide B derivative and the preparation method thereof, stability of the oral administration preparation composed of the bilobalide B derivative is improved.
WO2014142640A1 Improvements to the method for preparing hydroxocobalamin and the high-purity salts thereof The invention relates to a novel method for the production and purification of hydroxocobalamin and the pharmaceutically acceptable salts of same, wherein the method consists in converting cyanocobalamin into hydroxocobalamin by reduction, and the subsequent purification thereof, which produces better yields, prevents degradation of the hydroxocobalamin and substantially improves the purity of same and the salts thereof.
US20050020519 Increase concentration of peptide; controlling glucose uptake into cells; adjust metabolism; stimulate cell proliferation; reduce apoptosis; moderate gene expression' The invention relates to modulators of insulin-regulated aminopeptidase (IRAP)/Angiotensin IV receptor (AT4) activity, which have the ability to (a) increase local concentration of a wide range of peptides, thereby enhancing the activity of these peptides; (b) regulate glucose uptake into cells and tissues, thereby altering the metabolic or energy status of the cells or tissues; (c) trigger second messenger or signalling pathways associated with IRAP/AT4 function; and/or (d) increase cell surface expression of IRAP/AT4. The modulators may enhance learning and memory in both normal subjects and those with memory disorders. They also stimulate cellular proliferation while reducing apoptosis, thus stimulating tissue growth development, and affect angiogenesis. Thus they are also useful in tissue repair and regeneration. The invention also relates to methods of identifying modulators of insulin-regulated aminopeptidase activity.
US20080249073 Skin Treatment Composition This invention relates to a cosmetic composition comprising: a) Salicyloyl-sphingoidbases and/or derivatives thereof and b) a dermatologically acceptable carrier for treating and/or preventing cellulitic skin by increasing dermal structural proteins (collagen and fibrillin) and reducing the levels of MMP-1 activity.
EP1932526A1 Morin, a new inhibitor of microbial hyaluronate lyase This invention relates to a new inhibitor of microbial hyaluronate lyase and its use. The task of the invention to provide a new inhibitor of microbial hyaluronate lyase and to specify its applications is solved by using the flavonol morin as the inhibitor and by manufacturing pharmaceutical and cosmetic formulations that contain morin.
CN103301124A Medicine composition for treating epilepsy The invention relates to a composition for treating epilepsy, belonging to the technical field of medicines. The invention provides a compound medicine composition for treating epilepsy. The composition is characterized in that the composition contains 3,4-dichlorophenyl-propenoyl-sec.-butylamine and a sulfonamide carbonic anhydrase inhibitor; and the sulfonamide carbonic anhydrase inhibitor is selected from one of acetazolamide and zonisamide. The composition is provided to improve the compliance of patients and achieve the aim of controlling epileptic seizure, and simultaneously reduces the side effects of a clinical medicine of a central nervous system inhibitor. A safe and effective clinical medicine is provided for epilepsy patients.
EP2570407A1 Tetrazole-substituted arylamide derivatives and their use as P2x3 and/or P2x2/3 purinergic receptor antagonists Benzamide compounds or pharmaceutically acceptable salts thereof for treating diseases associated with the P2X3 and/or a P2X2/3 receptor.
US20060122181 Heteroaromatic pentacyclic compound and medicinal use thereof A 5-membered heteroaromatic ring compound represented by the formula [I] wherein V is CH or N; W is S or O; R1 and R2 are each H etc.; X is —N(R4)—, —O—, —S—, —SO2—N(R5)—, —CO—N(R7)— etc.; L is wherein R20, R21, R22 and R25 are each H etc.; E is aryl or heteroaromatic ring group; R is —COOH etc.; B is aryl etc.; R3 is H etc.; Y is —C(R13)(R14)—N(R12)—C(R13)(R14)—O—, —N(R11)—, —O— etc.; A is alkylene; and Z is aryl etc., a prodrug thereof and a pharmaceutically acceptable salt thereof. The compound [I] has a superior protein tyrosine phosphatase 1B inhibitory activity and is useful as a therapeutic agent for diabetes, diabetic complications, hyperlipidemia, obesity and the like.
US20120283194 Inhibitors of Atypical Protein Kinase C and Their Use in Treating Hedgehog Pathway-Dependent Cancers Methods and compositions are provided for modulating Hedgehog (Hh) pathway signaling in a cell. Aspects of the methods include methods for inhibiting Hh pathway-promoted cancer proliferation and/or metastasis that is promoted by Hh pathway signaling, methods for treating cancers promoted by Hh pathway signaling, and methods for screening candidate agents for the ability to treat a cancer promoted by Hh pathway signaling. In addition, reagents and kits thereof that find use in practicing the subject methods are provided.
WO2011151701A1 6 - methyl - 4 - phenyl - 5 - ( phenyl or cycloalkyl) carbamoyl - 1,2,3, 4 - tetrahydropyrimidin- 2 - one derivatives as antitubercular agents The present invention discloses antitubercular compounds selected from tetrahydropyrimidones/ tetrahydrothiopyrimidone derivatives of Formula (1) and its pharmaceutically acceptable salts for the treatment of Mycobacterium in the dormant phase. Formula (1) wherein, R is H, halogen, dihalogen, O-alkyl, di- O-alkyl, R1 is phenyl, chlorophenyl, nitrophenyl, diclorophenyl, cycloalkyl, preferably cyclohexyl, X is O or S.
WO2012175735A1 A20 inhibitors for the treatment of respiratory viral infections The present invention relates to the field of medicine, more particularly to the field of viral pneumonia. The invention shows that inhibition of A20 in respiratory epithelium and also the inhibition of A20 in alveolar macrophages results in an accelerated clearance of virus infected lungs. Accordingly, the invention provides for inhibitors of A20 and their use for the treatment of viral infections, more particularly viral lung infections such as influenza.
EP2731597A2 Methods for treating inflammation and hypertension with gamma-ketoaldehyde skavengers A method of treating at least one of inflammation, psoriasis, and/or hypertension comprising administering to a patient in need there of an effective gamma-ketoaldehyde scavenging amount of a gamma-ketoaldehyde scavenging compound.
WO2008018655A1 Novel thiazole-based compound and inhibitor of t-type calcium channel containing the same The present invention relates to novel thiazole-based compounds and T- type calcium channel inhibitors containing the compound. The T-type calcium channel inhibitor of the present invention is useful as a treating agent for disease associated with overexpression of T-type calcium channel.
EP1307198A4 Protoberberine derivatives which inhibit activity of the mitogen-activated protein kinase The present invention relates to protoberberine derivatives which inhibit the activity of mitogen-activated protein kinase. More specifically, the present invention is directed to protoberberine derivatives which inhibit the activity of Wis1 and Spc1 kinase in intracellular signal transduction cascade wherein mitogen-activated protein kinase (MAPK) is involved.
CN103181916A Venlafaxine hydrochloride slow-release capsule and preparation method thereof The invention relates to a venlafaxine hydrochloride slow-release capsule and a preparation method thereof. A drug-containing core of the slow-release capsule comprises venlafaxine hydrochloride, microcrystalline cellulose, gas phase silica, Tween-80, and hydroxypropyl methylcellulose; a slow-release coating comprises polyacrylic resin, talcum powder, polyethylene glycol and lauryl sodium sulfate. The invention realizes a pure water system for the capsule production by the addition of gas phase silica to change material flowing, and the selection of slow-release coating. The venlafaxine hydrochloride slow-release capsule prepared by the system is stable in drug release, has effective continuous release time of 24 hours, and is taken only once a day. The method is simple in process, mild in condition, free of any organic solvent, low in equipment requirements, and suitable for industrial production.
CN102614218A Crystal unit prepared through healing stone fusion and fusion method thereof The invention relates to a crystal unit prepared through healing stone fusion and a fusion method thereof. The crystal unit comprises crystobalite, nepherite grains and magnetite. Healing stones are placed into a stove and are fused, then molten state healing stones are led out of the stove, naturally cooled, and are magnetized to form the crystal unit prepared through healing stone fusion. The crystal unit can enable a quantized value of a crystal unit field to reach a value ranging from 13000 to 14000. The crystal unit is worn to improve human body biological fields, enables life elements to be correctly expressed, and gives life the largest power.
US20110044931 Multi-conjugate of sirna and preparing method thereof The present invention relates to a multi-conjugate of small interfering RNA (siRNA) and a preparing method of the same, more precisely a multi-conjugate of siRNA prepared by direct binding of double stranded sense/antisense siRNA monomers or indirect covalent bonding mediated by a cross-linking agent or a polymer, and a preparing method of the same. The preparing method of a siRNA multi-conjugate of the present invention is characterized by simple and efficient reaction and thereby the prepared siRNA multi-conjugate of the present invention has high molecular weight multiple times the conventional siRNA, so that it has high negative charge density, suggesting that it has excellent ionic interaction with a cationic gene carrier and high gene delivery efficiency.
EP1699797B1 Pyrrolotriazine compounds as kinase inhibitors The present invention provides compounds of formula (I); and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
US20110201644 Crystalline form of a benzimidazole-carboxamide medicinal compound The invention provides crystalline forms of the novel benzimidazole-carboxamide 5-HT4 receptor agonist compound, 4-(4-{[(2-isopropyl-1H-benzoimidazole-4-carbonyl)amino]methyl}-piperidin-1-ylmethyl)piperidine-1-carboxylic acid methyl ester. The invention also provides pharmaceutical compositions comprising the crystalline compound, methods of using the compound to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing crystalline forms of the compound.
CN102000082A Medicament or health care food with memory strengthening effect The invention discloses a medicament or a health care food with memory strengthening effect. A prescription of the invention comprises the effective components of DHA, taurine, zinc gluconate, vitamin B1, vitamin B2 and vitamin B6. Proved by meal test, the invention can certainly and effectively strengthen memory, has high taking safety and is suitable for long-term use.
WO2010060955A1 Novel 2-morpholino-3-amido-pyridine derivatives and their medical use The present application discloses novel 2-morpholino-3-amido-pyhcline derivatives and their use as modulators of the voltage gated KV7 (KCNQ) potassium ion channels in the treatment of pain, neurodegenerative disorders, urinary incontinence, etc... In other aspects the application discloses the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising these compounds.
CN1985842A Oral azithromycin resin suspension and its preparing method The present invention discloses a kind of oral azithromycin resin suspension and its preparation process, and aims at making the suspension possess good taste. The oral azithromycin resin suspension consists of in each 100 ml azithromycin 0.25-4.0 g, ion exchange resin 0.5-8.0 g and water for the rest. Its preparation process includes the following steps: mixing azithromycin, inorganic acid and/or organic acid and pure water; adding ion exchange resin to obtain mixed liquid; preparing suspension medium with suspending agent, surfactant and pure water; adding metal ion complexing agent, preservative, corrective and colorizing agent; adding the mixed liquid. The present invention is superior to available technology in that the oral azithromycin resin suspension has the bitter of azithromycin masked by the ion exchange resin and thus good taste.
CN102784135A Application of equol-based BKCa channel activation The invention discloses an application of equol-based BKCa channel activation. Pharmaceutical activity of equol is detected on the basis of applying a rat focal cerebral ischemia reperfusion model, a tail-cuff method to measure rat blood pressure, a Laser Doppler Flowmetry to observe brain parenchyma and pia mater blood flow, an in-vitro vascular muscle tension tracing and a patch clamp technology, and results show that the equol, through activating beta1 subunit of BKCa channel, can dilate blood vessels, increase cerebral blood flow and protect ischemic reperfusion brain tissue, is beneficial for prevention and treatment of ischemia brain stroke, and can be used for preparation of related medicaments.
DE102007015824A1 Agent, useful for the treatment of udder mastitis in mammals, preferably dairy cattle and of breast mastitis in humans, comprises an aqueous solution of N-chlorotaurine or its salt, preferably sodium salts Agent for the treatment of udder mastitis in mammals and of breast mastitis in humans, comprises an aqueous solution of N-chlorotaurine or its salt. An independent claim is included for the treatment of udder mastitis in mammals and of breast mastitis in humans, comprising instilling the agent with a cannula through the teats of the udder and nipples of the human breast in to the mammary gland. - ACTIVITY : Antiinflammatory. - MECHANISM OF ACTION : None given.
CN102731476A Benzo-cycloheptyl-pyridine derivatives containing cyanoguanidine structure, preparation method, and pharmaceutical compositions and medicinal application thereof The invention relates to compounds as represented by general formula (I) and pharmaceutically acceptable salts thereof. The compounds have good anti-allergic/anti-inflammatory effects. The invention also relates to a preparation method for the compounds and medicinal preparations containing the compounds. According to the invention, a series of the compounds as represented by general formula (I) and the pharmaceutically acceptable salts thereof are synthesized.
WO2011113862A1 Imidazopyrazines The present invention relates to imidazopyrazine compounds of general Formula (I) : in which X, R1, R2, R3a, R3b, R4a, R4b, R4C, and R4D are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
US20120190727 Method and means for treatment of osteoarthritis The present invention relates to in vivo and in vitro methods, agents and compound screening assays for inducing anabolic stimulation of chondrocytes, including cartilage formation enhancing pharmaceutical compositions, and the use thereof in treating and/or preventing a disease involving a systemic or local decrease in mean cartilage thickness in a subject.
WO2012098495A1 Pharmaceutical composition that includes revamilast and a beta-2 agonist The present patent application relates to a pharmaceutical composition that includes a PDE4 enzyme inhibitor, namely revamilast, and a beta- 2 adrenergic receptor agonist; a process for preparing such a composition; and its use in treating a respiratory disorder in a subject.
WO2012065527A1 Compouds and uses as l-type calcium channel blocker and/or acetylcholinesterase inhibitor thereof Disclosed in this invention are compounds and the uses as L-type calcium channel blocker and/or acetylcholinesterase inhibitor thereof. The uses of said compounds in the manufactures of a medicament for the treatment of cardiovascular diseases, apoplexy or senile dementia are also disclosed in the present invention.
CN103550167A Enrofloxacin effervescent granules for livestock and poultry and preparation method thereof The invention relates to enrofloxacin effervescent granules for livestock and poultry and a preparation method thereof. The enrofloxacin effervescent granules consist of the following raw materials and auxiliary materials in parts by weight: 60-120 parts of enrofloxacin, 80-140 parts of citric acid, 150-180 parts of sodium hydrogen carbonate, 20-40 parts of polyethylene glycol 6000, 190-260 parts of dextrin and 300-400 parts of sucrose. The preparation method comprises steps of respectively grinding the raw materials and auxiliary materials, mixing, granulating, drying, finishing and sub-packaging. The effervescent granules, depending on a veterinary medicine good manufacturing practice (GMP) standard, are good in curative effect, safe and reliable and researched and prepared by modern detection means and modern pharmaceutical equipment; the effervescent granules, which are added with the auxiliary materials and an effervescent disintegrating agent in the raw materials, are applied to diseased livestock and poultry through oral administration, and the effervescent granules are good in taste, stable in quality and high in medicine bioavailability.
CN101152556A Medicine liqueur with function of strengthening muscles and bones, method of preparing the same The invention provides a medicinal liquor with the function of strengthening tendons and bones and a method of preparing the liquor. The invention includes components, such as ginseng, barbary wolfberry fruit, english walnut seed, zingiber, etc., which are soaked into a container; the soakage liquid is evenly mixed and the product is obtained. The liquor is soaked by components. According to the pharmacology, different soaking time can better improve the medicinal effect. The medicinal liquor is externally applied on the skin, absorbed by the skin and acupoints, and directly functions on the nidus, with obvious effect in curing joints and caring entrails.
US20100279327 Method of treating diseases with parp inhibitors The present invention relates to methods of identifying a disease treatable with PARP modulators by identifying a level of PARP in a sample of a subject, making a decision regarding identifying the disease treatable by the PARP modulators wherein the decision is made based on the level of PARP. The method further comprises of treating the disease in the subject with the PARP modulators. The methods relate to identifying up-regulated PARP in a disease and making a decision regarding the treatment of the disease with PARP inhibitors. The extent of PARP up-regulation in a disease can also help in determining the efficacy of the treatment with PARP inhibitors. The present invention also relates to methods of identifying a disease treatable with PARP modulators by identifying a level of PARP in a plurality of samples from a population, making a decision regarding identifying the disease treatable by the PARP modulators wherein the decision is made based on the level of PARP. The method further comprises of treating the disease in a subject population with the PARP modulators. The methods relate to identifying up-regulated PARP in a disease and making a decision regarding the treatment of the disease with PARP inhibitors. The extent of PARP up-regulation in a disease can also help in determining the efficacy of the treatment with PARP inhibitors. The present invention discloses various diseases that have up-regulated or down-regulated PARP and can be treated with PARP inhibitors or PARP activators, respectively. The examples of the diseases include cancer, inflammation, metabolic disease, CVS disease, CNS disease, disorder of hematolymphoid system, disorder of endocrine and neuroendocrine, disorder of urinary tract, disorder of respiratory system, disorder of female reproductive system, and disorder of male reproductive system.
WO2010097576A1 1, 4-disubstituted piperidines as vasopressin receptor via antagonists The present invention provides compounds of formula (1) compositions comprising such compounds; the use of such compounds in therapy (such as in the treatment of dysmenorrhoea); and methods of treating patients with such compounds; wherein A and G are as defined herein.
US20080312314 Alpha crystalline form of strontium ranelate Alpha crystalline form of strontium ranelate of formula (I): characterised by its powder X-ray diffraction diagram and by a water content of from 22 to 24%. Medicinal products containing the same which are useful in the treatment of osteoporosis and arthrosis.
US20080306131 Progesterone receptor modulator and uses thereof Compounds of the structure: are provided. Also provided are methods of using these compounds as progesterone receptor modulators. Also described are methods of producing these compounds from a Verticillium species.
US20110136888 Substituted 1,3-Diphenylpropane Derivatives, Preparations and Uses Thereof The present invention involves substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, in particular in the fields of human and animal health.
US20130052190 CRTH2 Antagonists for Treatment of Eosinophilic Diseases and Conditions The present invention provides a method for the treatment of allergic and inflammatory diseases or conditions by administering a compound of Formula (I). The invention provides a method of treatment that is particularly suited for patients with a high degree of airway eosinophilia in contrast to those with a lower degree of airway eosinophilia. The invention also provides a method of treatment that is particularly suited for patients with a high atopic status in contrast to those patients with a lower atopic status.
CN101367807A Sulfhydryl pyrrolidine formamido pyridine substituted penem derivant The present invention belongs to the technical field of medicine, and in particular relates to a penem derivative substituted by sulfhydryl pyrrolidine carbamoyl pyridine as shown in Formula (I), an acceptable salt thereof in pharmacy, an easily hydrolyzed ester thereof, an isomer thereof, a hydrate thereof, and a hydrate of ester or salt thereof; wherein, R<1>, R<2>, R<3>, R<4> , R<5> and R<6> are defined as in the specification. The present invention also relates to the preparation methods of the compounds, drug compositions of the compounds, and the application of the compounds in preparation of medicine which is used for treating and/or preventing infectious diseases.
EP1587474A2 Fluoroalkoxy-substituted 1, 3-dihydro-isoindolyl compounds and their pharmaceutical uses The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates solvates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds in mammals for treatment or prevention of diseases associated with PDE4.
EP0998288B2 Compositions containing capsaicin or capsaicin analogues and a local anesthetic Methods and compositions for treating pain at a specific site with an effective concentration of capsaicin or analogues thereof are described. The methods involve providing anesthesia to the site where the capsaicin or analogues thereof is to be administrered, and then administering an effective concentration of capsaicin to the joint. The anesthesia can be provided directly to the site, or at remote site that causes anesthesia at the site where the capsaicin is to be administered. For example, epidural regional anesthesia can be provided to patients to which the capsaicin is to be administered at a site located from the waist down. By pretreating the site with the anesthetic, a significantly higher concentration of capsaicin can be used. Effective concentrations of capsaicin or analogues thereof range from between 0.01 and 10 % by weight, preferably between 1 and 7.5 % by weight, and more preferably, about 5 % by weight. This provides for greater and more prolonged pain relief, for periods of time ranging from one week to several weeks. In some cases the pain relief may be more sustained because the disease that underlies the pain may improve due to a variety of factors including enhancement of physical therapy due to less pain in the soft tissues which may foster enhanced mobilization of soft tissues, tendons, and joints.
CN101357923A Dipeptidase inhibitor compound The invention belongs to the medicine technology field, which more particularly relates to a dipeptidase inhibitor compound, the salt acceptable in pharmacy and the isomer thereof shown in the formula (I); wherein, the R<1>, Ar, X, m and n are defined in an introduction; The invention also relates to preparing methods of the compounds, the drug combination containing the compounds and the applications of the compounds in preparing the medicine for curing or preventing diabetes, non-insulin-dependent diabetes, hyperglycemia and insulin resistance.
US20130041028 Methods of using (1s,3s)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (1S,3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid also known as CPP-115 or its pharmaceutically acceptable salts can be used to treat addiction and neurological disorders such as epilepsy without side effects such as visual field defects caused by vigabatrin (Sabril).
CN103041013A Medicament for preventing and treating cutaneous henpox and preparation method thereof The invention discloses a medicament for preventing and treating cutaneous henpox. The medicament is characterized by being prepared from the following raw materials in parts by weight: 0.5 parts of fresh pepper, 0.3 parts of dry pepper and 5-7 parts of amoxicillin. According to the medicament, the fresh pepper and the dry pepper are boiled to prepare pepper water, a small amount of amoxicillin is added, and the mixture is drunk by chicken. The experiment shows that the medicament can be used for effectively preventing the cutaneous henpox, and effectively curing the cutaneous henpox when the chicken infects with the cutaneous henpox, wherein the cure rate is more than 95%. The raw materials are low in price, and easy to take, and the medicament is simple in preparation process and good in preventing and treating effects, so that the treatment cost for preventing and treating the cutaneous henpox can be effectively reduced, and the economic benefit of farmers can be increased.
CN102920717A Applications of stachyose in hangover alleviating The invention discloses new uses of a plant extract stachyose in hangover alleviating, wherein the stachyose is a stachyose product extracted from stachys sieboldii, stachys floridana schuttl.ex benth, stachys sieboldii, trumpetweed, soybean or rehmannia. According to the present invention, ordinary food, health food or medicine having a hangover alleviating function can be prepared by using the stachyose, and the hangover alleviating product comprises 1.0-100% of stachyose, 0.0-50% of a lobed kudzuvine root extract and 0.0-50% of a ethanol oxidase, can further comprises other additives, can be used before or after wine drinking, provides effects of protection of gastrointestinal tract, reduction of damage on liver by ethanol, and comprehensive adjustment of human internal environment, and is a health partner for drinkers.
CN103463031A Application of Lycojaponicumin B in medicine for promoting insulin secretion The invention belongs to the field of pharmacy, and discloses an application of Lycojaponicumin B in preparation of a medicine for promoting insulin secretion. The application of the Lycojaponicumin B in preparation of the medicine for promoting insulin secretion, disclosed by the invention, is disclosed for the first time. The skeleton type of the Lycojaponicumin B belongs to new skeleton type, and the insulin secretion promoting activity of the Lycojaponicumin B is unexpectedly strong, so that no possibility for providing any inspiration by other compounds exists. The Lycojaponicumin B has prominent substantial characteristics, meanwhile, has a remarkable progress in prevention and treatment of type 2 diabetes.
CN103102259A Ibuprofen hydrate crystal, medicinal composition containing hydrate crystal and preparation method thereof The invention relates to an ibuprofen hydrate crystal, a medicinal composition containing the hydrate crystal and a preparation method thereof. The molecular formula of the hydrate crystal is C13H18O2,H2O, and the characteristic peaks in the X-ray powder diffraction spectrogram are displayed when 2theta is 6.8 degrees, 11.4 degrees, 12.0 degrees, 12.8 degrees, 14.8 degrees, 15.9 degrees, 17.9 degrees, 19.4 degrees, 20.0 degrees, 21.6 degrees, 23.4 degrees, 24.2 degrees, 24.8 degrees and 30.6 degrees. The ibuprofen hydrate crystal improves the solubility of ibuprofen to some extent. The ibuprofen injection containing the crystal has favorable stability and fewer insoluble particles after being compounded with several injections, and thus, can completely satisfy the requirements in Chinese Pharmacopoeia, 2010 Edition. After compounding and standing for 4 hours, the insoluble particles can still completely satisfy the requirements in Chinese Pharmacopoeia, 2010 Edition.
WO2014138302A1 Quinazolinone antibiotics A new class of antibiotics effective against methicillin-resistant Staphylococcus aureus (MRSA) is disclosed. Compounds of this class can impair cell-wall biosynthesis by binding to both the allosteric and the catalytic domains of penicillin-binding protein (PBP) 2a. This class of antibiotics holds promise in reversing obsolescence of staphylococcal PBPs as important targets for antibiotics. Embodiments of the invention thus provide novel antibacterial compounds that target penicillin-binding proteins and/or other important cellular targets. Methods for inhibiting the growth and/or replication of bacteria using the compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, including drug-resistant strains of Staphylococcus aureus.
CN102247364A Compound medical application and preparation thereof The invention discloses a compound medical application, belonging to the technical field of medicaments. The invention specifically discloses an application of N-(2-methoxy ethyl)-2-(-3-nitro-1,2,4-triazole-1-) acetamide in preparing medicament capable of treating low immunity. The pharmacological test proves that the compound has good action on regulating immunity.
CN101511793A Antitumor agent for undifferentiated gastric cancer A compound represented by the General formula (I), a pharmacologically acceptable salt thereof, or a solvate of the compound or the salt can exert its effect more effectively on undifferentiated gastric cancer, and can also exerts its effect more effectively on a living body having at least one member selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing mutant FGFR2.
CN101648010B Preparation for promoting fibroblasts to secrete extracellular matrix components and preparation method thereof The invention discloses a preparation for promoting fibroblasts to secrete extracellular matrix components, and a preparation method and application thereof. The preparation comprises the components of A) the egg white of eggs, B) egg white lysozyme, and C) pyruvic acid or pyruvate, can also comprise ovotransferrin and/or glucose, and is obtained by mixing the components uniformly. The preparation can serve as an externally used paste for skin in application, and can obviously stimulate the secretion of collagen and hyaluronic acid synthase in the fibroblasts of the skin and improve the resiliency and the moisture content of the skin. The preparation is derived from a biologic extractive technique, has no harmful substance residues, safe and high-efficiency use, and is different from the prior method for promoting the secretion of a single fibroblast ECM component; besides, the preparation has multiple effects, wide application range and extensive application prospect, and can be applied in the fields of the preparation of skin substitutes, the preparation of anti-aging skin care products, cosmetics, medical treatment and the like.
WO2013081284A1 Complex antibacterial composition for animals The present invention relates to a complex antibacterial composition for animals, and more particularly, to a complex antibacterial composition containing enrofloxacin, trimethoprim, and sulfamethoxazole in a complex manner, thereby ensuring safe administration and also exhibiting remarkable effects on both a gram negative strain and a gram positive strain, pathogens of a bacterial digestive disease and a respiratory disease.
CN1931156A Nanometer solid taxol lipoid particle and its prepn process The present invention provides one kind of nanometer solid taxol lipoid particle capable of being used for injection and oral taking and its solid preparation, and features that taxol matter is coated with carrier material and surfactant so as to prepare nanometer solid taxol lipoid particle with small size, high coating rate, high stability, low toxicity and easy surface modification. The nanometer solid taxol lipoid particle has raised targeting effect on cancer cell, enhanced tumor cell killing effect, high curative effect, less toxic side effect, and reduced medicine resistance. The present invention also provides several preparation processes of nanometer solid taxol lipoid particle, and the preparation processes are simple, low in cost and suitable for industrial production.
WO2014086664A1 Substituted triazole boronic acid compounds The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
US7615562 Such as 2-methyl-4-{5-[2-(2,2,6,6-tetramethyl-piperidin-4-ylamino)-pyrimidin-4-yl]-thiophen-2-yl}-butan-2-ol; tumor necrosis factor inhibitors; immunosuppressants; antiinflammatory agents A compound of formula I or a pharmaceutically acceptable salt, ester or prodrug thereof wherein the variables have the meanings as defined in the specification. Further disclosed are a method of inhibiting IKK activity using a compound of formula I, a method of inhibiting production of TNF using a compound of formula I, a compound of formula I for use as a pharmaceutical, a pharmaceutical composition comprising a compound of formula I, and use of a compound of formula I in the manufacture of a medicament for use as an immunosuppressant or anti-inflammatory agent.
EP1809330B1 Compositions for reducing toxicity of cisplatin, carboplatin, and oxaliplatin The present disclosure is related to clear aqueous solutions of one or more bile acids and either an aqueous soluble starch conversion product or a non-starch polysaccharide. Solutions of the disclosure may be administered to a subject in conjunction with a pharmaceutical compound having one or more toxic effects. In some embodiments, solutions of the disclosure are administered to a mammal in conjunction with a pharmaceutical compound associated with a peripherial neurotoxicity (e.g., cisplatin and/or suramin) to reduce or eliminate the neuropathic effect(s).
US20100144775 Heterocyclic Cyclopamine Analogs and Methods of Use Thereof The present invention relates to steroidal alkaloids that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.
CN101991570A Stable compound keto acid preparation and preparation method thereof The invention relates to a stable compound keto acid preparation and a preparation method thereof. The compound keto acid preparation comprises keto acid calcium salt and amino acid, wherein one or more of the keto acid calcium salt and the amino acid respectively comprise a coating layer. Due to the prescription, the keto acid calcium salt or amino acid needed to be coated is respectively coated, and the keto acid calcium salt or amino acid is respectively pelletized so as to prepare compound keto acid granules, tablets or capsules. The preparation can be used for treating chronic kidney diseases, and has the characteristics that the preparation has stable quality, is difficult to decompose and easy to store and the like.
US8680096 Diphenyl-pyrazolopyridine derivatives, preparation thereof, and use thereof as nuclear receptor not modulators The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3.
US6900224 Effective against a broad range of pathogenic microorganisms with advantages in low susceptibility to microbial resistance, reduced toxicity, and improved pharmacology. Compounds of the following formula: are effective antimicrobial agents.
EP1578418A2 Use of substituted 2,5-diamidoindoles for the treatment of urological diseases The present invention relates to the use of 2,5-diamidoindole derivatives for the preparation of medicaments for treating urological disorders in humans and/or animals, by virtue of their endothelin-converting enzyme (ECE) inhibitory activity.
US20090203587 Diagnosis and Therapy of Cell Proliferative Disorders Characterized by Resistance to Trail Induced Apoptosis Described are methods and compounds for diagnosis and therapy of subsets of cell proliferative disorders which are characterized by resistance to TRAIL induced apoptosis. Examples of such diseases are B-cell chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), and prostate cancer. Furthermore, methods for identifying drugs which are suitable for treatment of such diseases are described.
CN1990004A Gargle with bad breath expelling function The invention provides a gargle for dispelling foul breath which comprises borax, boracic acid, clove oil, coloring matter and distilled water, and is prepared through specific processes. The gargle has good treatment action for foul breath.
CN101829135A Injection preparation with citicoline sodium and inosine as active ingredients, and application thereof The invention relates to an injection preparation with citicoline sodium and inosine as active ingredients, and application thereof. The injection preparation is prepared from citicoline sodium and inosine as pharmaceutical active ingredients, and pharmaceutically acceptable auxiliary materials. The preparation comprises powder injections, large-volume injections (more than 50ml) and small-volume injections (less than 20ml). The citicoline sodium and the inosine are used as raw materials, a certain type and proportion of the auxiliary materials are added, and then the oral preparation is prepared by the technical method. The preparation can be used for treating diseases of cerebrovascular hysfunction, craniocerebral injury, dementia, Parkinson's syndromes, heart diseases and the like.
WO2006107059A1 Medicine for renal perfusion disorder A pharmaceutical that is useful for the prevention and/or treatment of renal impairments, such as nephritis and renal insufficiency. There is provided a medicine for renal perfusion disorder characterized by containing, as an active ingredient, any of dihydropyridine compounds of the general formula: (1) [wherein R1 and R2, identical with or different from each other, represent a hydrogen atom, nitro or a chlorine atom; R3 represents a hydrogen atom, a chlorine atom or a fluorine atom; and n is an integer of 6 to 8] or an optical isomer thereof.
WO2011130788A1 Combined method for improving the health of skin Methods for improving the health of the skin of a subject comprising administering an oral composition comprising resveratrol, a proanthocyanidin, grape skin extract and vitamin C; a first topical composition comprising glycolic acid, a Vibrio Alginolyticus ferment filtrate and a water lily extract; and a second topical composition comprising a yeast extract, essential fatty acids, moisturiser, a water lily extract, water-soluble vitamins and fat-soluble vitamins are described.
WO2011080593A3 Materials and methods for prevention and treatment of viral infections The subject invention provides a novel and advantageous method for preventing and treating viral infection. Specifically exemplified herein are therapeutic uses of forsythoside A and jacaranone, compounds isolated from traditional Chinese medicinal material such as Fructus fυrsythiae (Lian Qiao). Also provided is use of a Yin Qiao San composition for preventing and treating viral infection.
US20100291061 Process for making oligopeptides There is described a method of synthesising a family of oligopeptides of predetermined amino acid sequence, which together make up from 7 amino acids to the complete amino acid sequence of a target protein, which comprises: synthesising a nucleic acid construct which codes for a fusion protein composed of overlapping peptides derived from the desired portion of the target protein, interspersed with regions which code for protease cleavage sites, expressing the nucleic acid construct in a suitable expression vector, harvesting the fusion protein corresponding to the nucleic acid sequence, and digesting the fusion protein with a protease selective for the cleavage sites to generate the oligopeptides. The oligopeptides may be generated in vitro or in vitro and may be used as vaccines against viral infections and in epitope mapping.
US20050130935 Combination of a beta-2-adrenoceptor agonists and an aminosugars and their use for the treatment immunomodulatory disorders The invention relates to combinations of an aminosugar and a beta-2-adrenoceptor agonist, such as salbutamol, for the treatment of diseases associated with hypersensivity and inflamation, in particular hypersensivity skin diseases. The aminosugar is preferably a monosaccharide derivative.
WO2006044457A1 N-benzenesulfonyl substituted anilino-pyrimidine analogs The present invention relates to compounds of formula (I), wherein R1, R2, R3, R4, R5, and R6 are defined herein.
CN101933925A Huperzine A with abirritation and derivatives thereof The invention relates to a method for treating pain, functional pain syndrome or organic pain syndrome. The method is characterized in that a compound shown in the formula (I) or salts thereof are applied to relieving or treating the pain, the functional pain syndrome or the organic pain syndrome of mammalian, wherein R expresses NR1R2, NHC(O)OR3 and N=CR4R5; R1 expresses H and C1-6 alkyl, R2 expresses H and C1-6 alkyl, R3 expresses C1-6 alkyl, heterocyclic and aryl, R4 expresses H, C1-6 alkyl, heterocyclic and aryl, and R5 expresses H, C1-6 alkyl, heterocyclic and aryl.
US20110251260 NOVEL siRNAS AND METHODS OF USE THEREOF The invention relates to compounds, in particular siRNAs, which inhibit the expression of specific human genes. The invention also relates to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The present invention also provides a method of treating and/or preventing the incidence or severity of various diseases or conditions associated with the genes and/or symptoms associated with such diseases or conditions comprising administering to a subject in need of treatment for such disease or condition and/or symptom the compound or the pharmaceutical composition in a therapeutically effective dose so as to thereby treat the subject. The invention also provides antibodies which inhibit specified human polypeptides and pharmaceutical compositions comprising one or more such antibodies.
CN103127066A Application of Eryngiolide A in medicines curing rarefaction of bone caused by lack of antiestrogen The invention discloses a new use of Eryngiolide A for curing rarefaction of bone. The rarefaction of bone is an important disease damaging human health, with aging of population, rarefaction of bone patients gradually increase, the rarefaction of bone causes huge burden on society, medical treatment and economy. Although relative experts and scholars at home and abroad attach great importance to prevent and cure the rarefaction of bone, the rarefaction of bone still lacks effective curing medicines. The fact that the Eryngiolide A has evident rarefaction of bone resisting function is discovered through in vivo test. Experiment results show that the Eryngiolide A can inhibit strengthening of bone conversion rate caused by ovariectomizing, reduce bone destruction, meanwhile can improve blood calcium concentration, and is benefit for deposition of bones. The Eryngiolide A has therapeutic effect on the deposition of rarefaction of bone caused by lack of the antiestrogen, and has no estrogen side effect.
US20090215780 Preparation and Use of Aryl Alkyl Acid Derivatives for the Treatment of Obesity This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
CN102961323A Liquid preparation for increasing active closed-loop rate of camptothecin compounds as well as preparation method and applications of liquid preparation The invention relates to a preparation for increasing the active closed-loop rate of camptothecin compounds through simply adding polyethylene glycol. The liquid preparation is prepared from polyethylene glycol, camptothecin derivatives and a dispersion medium, wherein the polyethylene glycol is taken as an additive, the camptothecin derivatives are taken as medicament molecules, the dispersion medium is taken as a solvent, and the main body of the dispersion medium is water. The main additive is polyethylene glycol, and the medicament molecules are one or more of camptothecin, 10-hydroxycamptothecine, 9-nitrocamptothecin, 9-aminocamptothecin, 7-ethyl-10-hydroxycamptothecine, Topotecan, Irinotecan, Rubitecan, Exatecan, Belotecan, Karenitecin, Chimmitecan, Gimatecan, and the like. Through simply adding polyethylene glycol, the preparation can significantly improve the active closed-loop rate of camptothecin drugs, enhances the medicament effect, and can effectively reduce the general reaction of medicament, and therefore, the preparation is expected to be used in the cancer treatment of different stages.
EP1140786B9 Reductive alkylation of secondary amines with hydrosilane A novel process for the production of tertiary amines by reductive alkylation of second amine using hydrosilane and a Lewis acid is disclosed. The novel process has application in the preparationof imidazole-containing benzodiazepines, inhibitors of farnesyl protein transferase.
CN101278795A Pillow good for sleep and production method The invention discloses a sleeping pillow and a manufacturing method. The raw materials include tuber pinellia, rush, spina date seed, milkwort, vine of tuber fleeceflower, chinese arborvitae kernel and vermilion. The manufacturing method is that the medicinal powder is ground into coarse powder, the powder is put into a pillow made of a thin cloth and then the pillow is placed into a plastic paper pillowcase for sealing. The invention is used by taking off the pillowcase and placing the head close to the pillow. The invention is characterized by external treatment for internal diseases, simple use, low price, tangible benefits, safety and comfort, and reliable curing effect.
CN103288819A Salt of crinum asiaticum novacine derivative The invention relates to crinum asiaticum novacine and fumarate of a derivative or a pharmaceutically acceptable solvate and an application of poison bulb novacine in preparation of medicines for treating cancer.
US20080280841 Amorphous Telithromycin Compound The present invention relates to stable amorphous 3-De[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribohexopyranosyl)oxy]-11,12-dideoxy-6-O-methyl-3-oxo-12,11-[oxycarbonyl[[4-[4-(3-pyridinyl)-1H-imidazol-1-yl]butyl]imino]]erythromycin (telithromycin), methods for the preparation thereof, the use of stable amorphous telithromycin in the treatment of bacterial infections and to pharmaceutical compositions comprising stable amorphous telithromycin.
US7371846 Chemokine coreceptor fusion for use prevention and treatment of viral infection; immunotherapy The invention relates to novel CD4-independent HIV Envelope proteins and uses therefor.
US20090197858 Hypercholestrolemia and tendinous injuries This invention provides compositions and methods of inhibiting, suppressing, or treating a tendinous or musculoskeletal soft tissue injury. The invention further provides a method of ameliorating symptoms associated with a tendinous or musculoskeletal soft tissue injury. Additionally, the invention provides methods for evaluating the risk of developing a tendinous or musculoskeletal soft tissue injury.
WO2008013324A1 Use of diabetes-related, liver-derived secreted protein in diagnosis or treatment of type-2 diabetes or vascular disorder Disclosed is use of selenoprotein P in the diagnosis or treatment of type-2 diabetes or a vascular disorder. Specifically disclosed are: a method for detection of type-2 diabetes or a vascular disorder, comprising measuring selenoprotein P; a method for evaluation of the risk of being suffering from type-2 diabetes or a vascular disorder; a method for evaluation of the insulin resistance or blood glucose control in a subject; and a therapeutic agent for type-2 diabetes or a vascular disorder which is targeted to selenoprotein P.
CN102872024A Misoprostol medicine combination used in mouths The invention discloses a misoprostol medicine combination used in mouths. The misoprostol medicine combination can be used in mouths and is good in taste, can be dissolved, disintegrated and dispersed in the mouths without water drinking or can be disintegrated and dispersed by aid of mouth chewing and then be absorbed or swallowed in the mouths. The misoprostol medicine combination can be sublingual tablets, chewable tablets, mouth lozenges, mouth disintegrating tablets, mouth film agents and dropping pills, and preferably be the sublingual tablets, the chewable tablets, the mouth disintegrating tablets and the mouth lozenges. The medicine combination can be used for promoting uterine contraction and preventing and treating postpartum hemorrhage. The medicine combination is simple in dosing method, safe, efficient, capable of being accepted by people easily, simple in preparation process and suitable for industrial production.
EP0947584B1 Loxoprofen-containing preparation for external use Problem: to provide a favorable antiphlogistic/analgesic containing loxoprofen or a medically acceptable salt thereof. Means for resolution: an antiphlogistic/analgesic for external use containing loxoprofen or a medically acceptable salt thereof and crotamiton.
US20100311782 Substituted piperidinylpropanoic acid compounds and methods of their use Novel 3,4-disubstituted-4-(3-carbamoylphenyl)-piperidinylpropanoic acid compounds and their salts, including pharmaceutically acceptable salts, pharmaceutical compositions and methods of their use are disclosed. The novel compounds are useful, inter alia, as antagonists of opioid receptors.
US20070031443 Methods for treating or preventing skin disorders using CD2-binding agents Methods for treating or preventing an epidermal or dermal disorder, e.g., psoriasis, using a CD2-binding agent, e.g., an inhibitor of the CD2/LFA-3 interaction (e.g., an LFA-3/IgG fusion polypeptide), in combination with an auxiliary agent, e.g., UVB irradiation, are disclosed.
CN103315977A Folic acid modified quercetin lipid nano-capsule preparation and preparation method thereof The invention discloses a folic acid modified quercetin lipid nano-capsule preparation and a preparation method thereof. The preparation comprises the following components in parts by weight: 0.05-5 parts of quercetin, 15-60 parts of distilled water, 5-20 parts of medium chain triglyceride, 10-50 parts of polyethylene glycol monostearate, 0.05-5 parts of lecithin, folic-acid-polyethylene glycol-cholesteryl hemisuccinate and sodium chloride, wherein a folic acid lipid material accounts for 0.01-3 percent of the total weight of the preparation, and sodium chloride accounts for 1-3 percent of the total weight of the preparation. The grain size of the nano-capsule preparation is between 10 and 150nm, a used surfactant contains massive PEG (polyethylene glycol) chains, and the preparation in a body is prevented from being devoured by the reticuloendothelial system by virtue of the nano-grade grain size, a hydrophobic core and a hydrophilic shell; and the mode of intravenous injection plays roles in targeting, long circulating and the like, and is advantageous to clinical application of the preparation.
US20080227853 Administering catechin, epicatechin, and derivatives thereof; apoptosis; cancer; microencapsulation Disclosed is a method of treating or preventing a disorder influenced by the action of a membrane androgen receptor, wherein a patient suffering or expected of suffering of such disorder is administered in pharmaceutically effective amounts an agonist of the membrane androgen receptor, said agonist being selected among the group consisting of natural, unnatural, oligorimerised or rearranged catechin, epicatechin, and derivatives thereof. The disease being treated or prevented may be cancer.
US20110224216 Methods of Treating or Preventing Acute Erythema A method of treating or preventing acute erythema in a human in need thereof by topical administration of an effective amount of an alpha adrenergic receptor agonist or pharmaceutically acceptable salt thereof is claimed. The preferred alpha adrenergic receptor agonist is brimonidine. A method of preventing secondary inflammation caused by acute erythema by topical administration of an effective amount of an alpha adrenergic receptor agonist or a pharmaceutically acceptable salt thereof is also claimed.
WO2005003094A1 Diarylmethyl derivatives as potassium channel modulators This invention relates to novel compounds useful as potassium channel modulators. More specifically the invention provides chemical compounds useful as modulators of SKCA and/or IKCA channels.
CN102786535A Polymerization aaptamine alkaloid compounds, preparation method thereof and application of polymerization aaptamine alkaloid compounds The invention relates to the technical field of medicines, in particular to 7 novel dimerization and trimerization aaptamine alkaloid compounds having antineoplastic activity. The 7 novel dimerization and trimerization aaptamine alkaloid compounds are separated from sponge Aaptos suberitoides (1934) collected in the South Sea of China. Vitro antineoplastic activity experiments show that the alkaloid compounds has evident inhibition effect to tumor cells such as K562 (chronic myelocytic leukemia) and P388 (mouse leukemia cells) and can be used to prepare antineoplastic drugs. By the alkaloid compounds, lead compounds for researching novel antineoplastic drugs are provided, and development and utilization of marine medicinal resources are facilitated.
WO2008060581A3 Compositions including triciribine and trastuzumab and methods of use thereof This application relates to combination therapies including triciribine and related compounds and trastuzumab or a salt thereof and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
WO2010000353A1 Sulfonamides with heterocycle and oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to Sulfonamides with heterocycle and oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
WO2012064221A1 Drug for treating liver lesions caused by the action of chemical or biological agents The invention relates to medicine and can be used for treating liver lesions caused by chemical or biological agents. The drug for treating liver lesions caused by chemical or biological agents is comprised of 1-(4-bromophenyl)-6-hydroxy-5-nitroso-1,2,3,4-tetrahydropyrimidine-2.4-dione: (I), or salts thereof having the general formula: (II), where X is selected from Na+, К+, Li+, NH4 +, NH2CONH3 + or another pharmacologically acceptable cation. The effectiveness of the preparation in treating liver diseases of different etiologies is increased.
WO2011069053A1 Process for the preparation of pazopanip hcl and crystalline forms of pazopanib hcl Various crystalline forms of Pazopanib HCl were prepared. In preferred embodiments the obtained Pazopanib HCl is essentially free from CPMI.
EP1014990B1 Antitumor combination of 3-amino-1,2,4-benzotriazine 1,4-dioxide/paclitaxel/platinum In accordance with the present invention there is provided a method of treating a mammal having a solid tumor, the method comprising: a) administering to the mammal an effective amount of 3-amino-1,2,4-benzotriazine 1,4-dioxide; b) administering to the mammal an effective amount of paclitaxel; and c) administering to the mammal an effective amount of a platinum complex. The method provides unexpected synergistic efficacy. The invention further provides a kit for treatment of a mammalian tumor comprising 3-amino-1,2,4-benzotriazine 1,4-dioxide, paclitaxel and a platinum complex.
CA2803923A1 Methods of using sterculic acid The use of sterculic acid, and the pharmaceutically acceptable salt forms thereof, described for the treatment of inflammation, in particular, 7-ketocholesterol induced inflammation, 7-ketocholesterol toxicity, and unregulated angiogenesis.
CN103467516A Golden phosphorous acetyletic compound, and preparation method and applications thereof The invention discloses a golden phosphorous acetyletic compound in the general formula, and a preparation method and applications thereof. The golden phosphorous acetyletic compound has stronger in-vivo stability, and can efficiently and specifically inhibit the activity of thioredoxin reductase in a targeted manner, thus inhibiting the increase of tumor through damaging intracellular redox level; in addition, better in-vitro and in-vivo tumor inhibition effects can be achieved, the targeted tumor treatment effect can be realized, and the golden phosphorous acetyletic compound has wide application prospects.
US20100285111 Self-assembling micelle-like nanoparticles for systemic gene delivery Nanoparticles containing nucleic acid and suitable for use as in vivo delivery agents for nucleic acids are provided. The nanoparticles use a covalent conjugate of a polycation such as polyethylenimine and phospholipids. The final DNA-containing nanoparticle has a vesicular structure with a polyplex core surrounded by a mixed lipid/PEG-lipid monolayer envelope and offers simple preparation, high loading capacity, and in vivo stability. The nanoparticles have good in vivo stability and a prolonged blood circulation time and can effectively deliver a gene to a biological target such as a tumor.
US20050287159 Treatment methods for eotaxin mediated inflammatory conditons Immunogenic compositions which generate an active immune response in a subject comprising autoantibodies to eotaxim which neutralize its biological activity and treatment methods using such compositions.
CN103622971A Medicament composition for preventing and/or treating alzheimer diseases and application thereof The invention discloses a medicament composition for preventing and/or treating alzheimer diseases. The composition is composed of galanthamine and lycobetaine. The two medicaments in combination have excellent synergistic effects on inhibition of acetylcholin esterase activity and can be used for treating alzheimer diseases. By using the composition, the administration dosage of galanthamine can be greatly reduced when being used for preventing and/or treating alzheimer diseases, therefore, the side effects of a medicament are avoided and the administration compliance is improved.
EP0925065B1 Water miscible erythromycin compositions Water miscible pharmaceutical compositions containing up to about 40 % of erythromycin prepared by reaction with acetic acid in a non-aqueous water miscible organic solvent system.
EP1485145B1 Multiple compartment bag assembly containing dialysis fluid The invention concerns a multiple compartment flexible bag assembly including a first predetermined volume of an aqueous sodium bicarbonate component solution contained in at least one of the multiple compartments and a second predetermined volume of an aqueous acid component solution contained in at least another of the multiple compartments, the component solutions being intended to be mixed together to obtain a peritoneal dialysis, hemodialysis or replacement fluid, characterized in that the aqueous acid component solution comprises an amount of dissolved carbon dioxide. The partial pressure value of carbon dioxide exhibited the aqueous acid component solution is preferably matched with the partial pressure value of carbon dioxide determined for the aqueous sodium bicarbonate component solution.
US20120010276 Screening and therapy for lymphatic disorders involving the flt4 receptor tyrosine kinase (vegfr-3) The present invention provides materials and methods for screening for and treating hereditary lymphedema in human subjects.
EP1725228A2 Use of docosatrienes, resolvins and their stable analogs in the treatment of airway diseases and asthma The present invention is generally drawn to novel isolated therapeutic agents, termed resolvins, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenaseII (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful ;isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or trihydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.
CN101530587A Medicament for treating abasia and rheumatism The invention relates to a medicament for treating abasia and rheumatism, which is prepared from 24 grams of Chinese angelica, 24 grams of white paeony root, 21 grams of largehead atractylodes rhizome, 21 grams of poria, 24 grams of big white, 30 grams of eucommia bark, 30 grams of medicinal cyathula root, 30 grams of common monkshood mother root, 30 grams of kusnezoff monkshood root, 30 grams of dipsacus, 30 grams of speranskia, 24 grams of tsaoko amomum fruit, 24 grams of Chinese hydrangeavine root-bark, 10 grams of hairy antler, 24 grams of obscured homalomena rhizome, 30 grams of common clubmoss herb, 30 grams of common floweringquince fruit, 30 grams of nux vomica (stir-baked to yellowish by sand and unhaired), 1 gram of musk, 24 grams of fineleaf schizonepeta herb, 24 grams of divaricate saposhnikovia root, and 6 grams of camel hair by grinding into crude powder and sealing into 1,500 milliliters of grain wine for 7 days. The medicament is taken by a patient in 5 milliliters each time and twice per day. The formulation has the effects of promoting blood circulation by removing blood stasis, clearing and activating the channels and collaterals, expelling wind and removing the rheumatism and the like.
CN103446068A Bortezomib freeze-dried composition and preparation method thereof The invention belongs to the field of medicine and provides a bortezomib freeze-dried composition and a preparation method thereof. The bortezomib freeze-dried composition is a freeze-dried composition which is obtained through the steps of spraying the mixed solution of bortezomib, mannitol and tertiary butanol into liquid nitrogen to form frozen microparticles, dissolving the microparticles in water for injection, and finally, performing freeze-drying. The bortezomib freeze-dried composition provided by the invention is better in quality and higher in stability.
US20100087482 Method for Treating Gefitinib Resistant Cancer The present invention is directed to methods for the treatment of gefitinib and/or erlotinib resistant cancer. An individual with cancer is monitored for cancer progression following treatment with gefitinib and/or erlotinib. Progression of the cancer is indicative that the cancer is resistant to gefitinib and/or erlotinib. Once progression of cancer is noted, the subject is administered a pharmaceutical composition comprising an irreversible epidermal growth factor receptor (EGFR) inhibitor. In preferred embodiments, the irreversible EGFR inhibitor is EKB-569, HKI-272 and HKI-357.
CN102341092A Method of dissolving antifungal agent, and compositions with high concentration of antifungal agent, suitable for application to the nail The invention provides a pharmaceutical composition which comprises: an antifungal agent from the class of the allylamines or the morpholines, at a concentration of at least 5 %; a ternary solvent system comprising water; at least one branched or straight chain C2-C8 alkanol; at least one glycol; and the total amount of water representing more than 30 % (w/w) of the composition. This composition is intended for application to the nail for the treatment of onychomycoses.
EP1751150A2 Novel azabicyclic aryl derivatives This invention relates to novel azabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
US6858626 Cyclic hydroxamic acid as metalloproteinase inhibitors The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.
US20080160110 Anti-Aging Cosmetic Composition The present invention relates to an anti-aging cosmetic composition, and more particularly, the present invention relates to an anti-aging cosmetic composition containing Hibiscus esculentus extracts and at least one selected from the group consisting of oleanolic acid, ursolic acid, glycyrhetinic acid and retinol, showing high safety to skin and wrinkle-improvement effect.
EP1575594A2 Combination of reboxetine and a cyclooxygenase-2 inhibitor A method of treating, preventing, or inhibiting a CNS disorder and/or pain and inflammation, or an inflammation-associated disorder in a subject in need of such treatment, prevention, or inhibition provides for treating the subject with reboxetine and a cyclooxygenase-2 selective inhibitor or prodrug thereof, wherein the amount of reboxetine and the amount of a cyclooxygenase-2 selective inhibitor or prodrug thereof together constitute a CNS disorder and/or pain and inflammation or inflammation-associated disorder suppressing treatment, prevention, or inhibition effective amount of the composition. Compositions and pharmaceutical compositions that contain reboxetine and a cyclooxygenase-2 selective inhibitor are also disclosed.
EP2436762A1 Method for prediction of therapeutic effect of chemotherapy employing expression level of dihydropyrimidine dehydrogenase gene as measure The present invention provides an antitumor agent comprising cisplatin and a combination drug of tegafur/gimeracil/oteracil potassium that ensures an excellent life-prolongation effect in advanced gastric cancer patients that is superior to that of the standard therapy in Europe and the U.S. using an agent that contains 5-FU and does not contain a dihydropyrimidine dehydrogenase inhibitor, by way of selecting the patients based on dihydropyrimidine dehydrogenase.
CN1579412A Cytidine triphosphate disodium chloride injecta and its preparation process The invention is cytidine triphosphate di-sodium chloride injection and its manufacturing method. The product is apt to be polymerized in storing process, thus the anaphylactic response increases, in clinic, the product is dissolved in the 0.9% sodium chloride injection, it increases the probability of medicine being infected, affects the safety of medicine use, and it increase the working labor of medical care personnel. Its ingredients include: liquid, which includes cytidine triphosphate di-sodium, sodium chloride and water for injection, its weight shares are: cytidine triphosphate di-sodium 5-50, sodium chloride 300-1500, water for injection 100, pH value is 5.0-8.0. The product can be used to cure cerebral concussion and its sequela, neurosis and hepatitis and son on.
CN101278915A Medicament composition granule and method of preparing the same The invention relates to a medicinal composition particle containing omeprazole and a preparation method thereof; active ingredient is the medicinal composition particle containing the omeprazole, and also contains diluent, antacid, suspending agent, disintegrating agent, correctant and binder which are used as carrier for preparing particle.
WO2007101371A1 Preparation and use of purine bis-amino acid esters The invention provides purine bis-amino acid esters represented by formula (I), and pharmaceutically-acceptable inorganic or organic salts thereof, wherein R1 is an amino group; R2 is an amino-protected or free L-amino acid; n is 0 or 1; X is O or S. The invention also provides the preparation of such compounds and the use of such compounds as active substance in preparation of a medicament for the treatment of viral diseases. (I)
CN1948275A Verakanol Mannich alkali derivative, its preparation method and use The present invention belongs to the field of medicine technology, and discloses a resveratrol Mannich alkali derivative, its preparation method and application. Said invention uses 3,5-dihydroxy (or dialkoxyl)-4'-hydroxydiphenylethene, various substituted secondary amines and formalin solution (or paraformaldehyde) as raw material and makes them produce reaction in conventional solvent so as to prepare the invented compound resveratrol Mannich alkali derivative. Said invention also provides its chemical structure formula. Its medicinal free alkali and medicinal have good action for preventing and curing several diseases of tumor, angiocardiopathy and inflammation, etc.
EP1853606A1 Pyridopyrazolopyrimidine compounds and their uses as anti-cancer and anti-diabete drugs The present invention relates to pyridopyrazolopyrimidine derivatives that are useful pharmacological agents through the inhibition or antagonism of protein kinases, and to processes for the preparation and use of the same. In particular, the present invention relates to compounds that demonstrate protein tyrosine kinase and/or protein serine/threonine kinase inhibition.
WO2010087527A1 Ultraviolet absorbers, and pharmaceutical compositions and cosmetics containing pyrimidine compounds for uv protection The present invention provides new ultraviolet absorbers, and new pharmaceutical compositions and cosmetics containing pyrimidine compounds for UV protection and melanogenesis inhibition. The present invention also provides methods for making those agents. Those pyrimidine compounds are 2-substituted-6-alkyl-5-oxo- 5,6-dihydro(7H)pyrro[3,4~d]pyrimidine compounds, and 2-substituted-7-alkyl-6~oxo- 5,6-dihydro(7H)pyrro[2,3-d]pyrimidine compounds and salts thereof, represented by the following formula (1 ) or formula (2), wherein R1 to R8 independently represent a hydrogen atom, a lower alkyl (especially C1 -C7 alkyl) group, CH3OCH2CH2-, -CH2COR9(R9=CH3, C2H5. NH2), - CH2OCOC2H5; and X represents -N (RI0) - (R10=CH3, C2H5, Ph,-CH2Ph,-CH (Ph)2,-COCH3, -COOCH3,-SO2CH3),-CH2-,-CH (CH3) -,-CH (C2H5) -,-O-,-S- in which ph stands for a phenyl group.
US20120202875 Method Of Treatment The present invention relates to methods for treatment or prevention of autoimmune and inflammatory diseases and conditions by inhibiting or modifying histone demethylation. In a further aspect the invention relates to a method for identifying agents useful in said methods of treatment. The invention particularly describes the role of certain histone demethylase enzymes in these diseases and conditions and their use as therapeutic and screening targets.
CN101115742B Heterocycle derivatives as histone deacetylase (hdac) inhibitors The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.
WO2010148177A3 Compounds, compositions, methods of synthesis, and methods of treatment Embodiments of the present disclosure provide for chloride channel or transporter compounds or compositions (inhibitors or agents), methods of synthesizing these compounds or compositions, methods of treatment using these compounds or compositions, and the like.
CN102441052A Medicine used for treating impetigo The invention discloses a medicine used for treating impetigo, which is prepared from the following steps of: adding 2000ml of water into 30g of golden cypress, 10g of Coptis chinensis, 50g of astragalus mongholicus, 10g of rheum officinale, 20g of radix sophorae flavescentis and 20g of cortex dictamni, and decocting until the mixture is 200ml; then, deslagging the obtained product; decocting 200ml of medicine liquid with slow fire into paste; refining to obtain oil by eight cooked egg yolks; evenly stirring the medicine paste with the egg yolk oil; and obtaining 2-3g of borneol. The medicine has the efficacy on diminishing inflammation and sterilizing, and has the advantages of quick effectiveness and good curative effect, and the total effective rate is 98%.
WO2012067614A1 Periodontitis treatment The periodontitis treatment is a method for the prevention and treatment of periodontitis in mammals, including humans and dogs. The mammal may be diabetic or non-diabetic. the method includes the step of administering an effective amount of an aldose reductase inhibitor (ARI). The ARI may be (i) a phenolic derivative, such as quercetin, quercitrin (a 3-oxy-glucose analog of quercetin), rutin, and other polyphenols or bioflavonoids exhibiting an ARI effect; (ii) an acetic acid derivative, such as tolrestat, ponalrestat, etc.; (iii) a cyclic imide (or hydantoin), such as sorbinil, 2-methyl sorbinil, imirestat, etc.; and (iv) one of the phenylsulfonylnitromethtane derivatives, such as ZD-5522. In particular embodiments, the method may include, e.g., administering a diet containing about 0.08% quercetin (about 80 mg/kg/day), about 0.0125% imirestat (about 12 mg/kg/day), or about 0.015% tolrestat (about 20 mg/kg/day).
CN101856331B Arginine (s)-ibuprofen granules and preparation method thereof The invention discloses arginine (s)-ibuprofen granules which are prepared from the following raw materials in parts by weight: 1 part of arginine (s)-ibuprofen, 1-100 parts of fillers, 1-20 parts of adhesives, 0.2-10 parts of thickening agents and 0.1-10 parts of flavoring agents. The granules are quickly dissolved in water to form transparent liquid with good mouthfeel, are convenient to take and have high bioavailability. The preparation method is simple, dispenses with any special equipment and is suitable for industrial production.
WO2011118891A1 Pharmaceutical composition including sulfuretin or pharmaceutically acceptable salt thereof for prevention and treatment of nervous system disorder The present invention relates to a pharmaceutical composition including sulfuretin or a pharmaceutically acceptable salt thereof, and to a method for prevention or treatment of nervous system disorders using same. Furthermore, the present invention relates to a functional food composition, including sulfuretin or a pharmaceutically acceptable salt thereof, for improving nervous system disorders, which can be effectively used for the prevention and treatment of neurodegenerative brain disease, depression, and anxiety due to various nervous system disorders.
US20090099107 Methods and Compositions for Inhibition of Nuclear Factor kappaB A series of p105-based NF-κB super repressors, designated p-105(sr), have been designed. The p105(sr), no longer generates p50 and undergoes signal-induced degradation, effectively inhibiting all NF-κB activities. Additionally, p105(sr) significantly enhances tumor necrosis factor alpha (TNF-α)-mediated killing of MT1/2 skin papilloma cells when p50 homodimer activity is elevated. p105(sr) is an effective NF-κB super repressor with a broader range than other currently available IkBα super repressors. The novel repressor can be used in cells where a noncanical NF-κB activity is dominant or multiple NF-κB activities are activated.
WO2008030892A2 Drug design for tubulin inhibitors, compositions, and methods of treatment thereof The present invention relates to a computer-assisted method of a designing of a tubulin inhibitor comprising: a) determining an interaction between a tubulin protein and a chemical known to bind the tubulin protein by evaluating a binding of the tubulin protein to the chemical known to bind the tubulin protein; b) based on the interaction, designing a candidate tubulin inhibitor; c) determining an interaction between the tubulin protein and the candidate tubulin inhibitor by evaluating a binding of the tubulin protein to the candidate tubulin inhibitor; and d) concluding that the candidate tubulin inhibitor inhibits the tubulin protein wherein the conclusion is based on the interaction of step c). The invention also provides compositions and methods of treatment of diseases with the candidate tubulin inhibitors.
US20110257153 Aryl-substituted bridged or fused diamines as modulators of leukotriene A4 hydrolase Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.
CA2506850C Compounds and methods for increasing neurogenesis The invention is directed to methods of promoting neurogenesis by contacting neuronal tissue with intracellular cAMP elevating agents and intracellular Ca2+ elevating agents. Novel agents for promoting neurogenesis are disclosed. These agents include novel agents for increasing intracellular cAMP.
US20110009474 Sirtuin based methods and compositions for treating beta-catenin-related conditions Provided herein are methods and compositions relating to sirtuin modulation of Wnt pathway signaling, including the use of sirtuin and sirtuin-modulating agents in the prevention and treatment of cancer and other diseases.
CN102106843A Slow-release lung targeted microcapsule preparation of florfenicol and preparation method thereof The invention relates to a slow-release lung targeted microcapsule preparation of florfenicol with a good targeted function and a slow-release function, and a preparation method thereof. The capsule selects gelatin, ethyecellulose or arabic gum as a material, and the florfenicol micropowder as a capsule core, wherein the mass ratio of the material to the capsule core is controlled to be (1:1)-(1:2); and the particle size of the florfenicol micropowder is controlled to be 2-10 mu m. The preparation method comprises the following steps: swelling the capsule material in water in advance, wherein, the weight concentration is controlled to be 10-20%; evenly suspending the florfenicol micropowder into an aqueous solution of the capsule material; manufacturing a microcapsule through a spray drying method, wherein, the air intake temperature is controlled between 80 and 110 DEG C, the air outlet temperature is controlled between 110 and 130 DEG C, and the spray flow is 0.3-0.6 litre per minute; and performing spray drying to prepare the microcapsule preparation which has the lung targeted function, can lead drugs to enrich into lung tissues, has better curative effects on lung infection, has a long-acting and slow-release function, decreases the times of drug administration, lowers the quantity of labor of cultivation workers, and lightens the stress reaction of animals.
EP1542700B1 Zoledronic acid for preventing or reducing secondary fractures after hip fracture Use of a bisphosphonate in the preparation of a medicament for the treatment of osteoporosis post hip fracture to prevent or reduce subsequent osteoporotic skeletal fractures in a patient in need of such treatment, and particularly to a patient who has undergone recent repair of the hip fracture and corresponding methods of treatment.
US20090124639 valacyclovir formulations The present invention relates to valacyclovir formulations having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.
EP2721008A1 Hydroxy substituted isoquinolinone derivatives The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
EP1695704A1 Derivatives of aryl (or heteroaryl) azolylcarbinols for the treatment of fibromyalgia The present invention refers to the use of derivatives of aryl (or heteroaryl) azolylcarbinols of general formula (I), and their physiologically acceptable salts, as medicinal products for human and/or animal therapeutics for the treatment of the symptoms of fibromyalgia, the prevention or the prophylaxis of the symptoms of fibromyalgia, as well as the prevention or the prophylaxis of the disease causing the symptoms.
WO2005018608A1 Drug delivery system for sub-tenon’s capsule administration of fine grains It is intended to provide a continuous drug delivery system targeting a tissue in the posterior segment of eye which needs no frequent administration and shows little tissue invasion. Namely, a drug delivery system whereby a drug is selectively transferred into the posterior segment of eye, thereby lessening effects of the drug transfer on the anterior segment of eye. By administering fine grains containing a drug under Tenon’s capsule, a drug delivery system ensuring the selective transfer of the drug toward the posterior segment of eye and maintenance of an efficacious drug concentration can be constructed.
CN1650852A L-lysine bydrochloride aseptic powder agent for injection and its preparation method An aseptic powder injection of L-lysine hydrochloride is prepared through dissolving L-lysine hydrochloride in medical organic solvent or water, filtering by millipore film, cooling to educe out solid, adding medical organic solvent or water, stirring, cooling to educe out solid, washing with absolute alcohol, vacuum drying, and vacuum packing.
CN103623042A Application of lung-heat-clearing stonecrop medicine composition to preparation of anti-influenza A virus medicine The invention discloses application of a lung-heat-clearing stonecrop medicine composition to preparation of anti-influenza A virus medicine. The lung-heat-clearing stonecrop medicine composition is prepared from the following raw materials in weight part: 300 parts of rhodiola rosea, 300 parts of travertine, 200 parts of platycodon grandiflorum and 200 parts of liquorice. The lung-heat-clearing stonecrop medicine composition is a lung-heat-clearing stonecrop capsule or a pharmaceutical preparation which is prepared after the medicinal materials in a prescription are prepared into active ingredients, and the pharmaceutical preparation can be a sugarcoated tablet, a thin membrane coated tablet or a capsule preparation. The pharmacological experiments show that the lung-heat-clearing stonecrop medicine composition has a certain inhibition effect on influenza A in vitro and in vivo, can remarkably inhibit the influenza A virus-induced pulmonary index increase in miceinhibit the influenza A virus-induced pulmonary index increase in mice, remarkably inhibit the influenza A viruses to reduce immune organs in mice, remarkably prevent the influenza viruses from killing the mice, and has a significant regulating effect on hypoimmunity caused by virus infection. Moreover, the protective effect of the lung-heat-clearing stonecrop medicine composition prepared by a novel process is commensurate with that of virazole.
US20090012027 Biodegradable polyphosphoramidates for controlled release of bioactive substances The present invention is directed to a series of new polycationic biodegradable polyphosphoramidates. Process for making the polymers, compositions containing these polymers and bioactive ligands to enhance the cellular uptake ad intracellular trafficking, articles and methods for delivery of drugs and genes using these polymers are described. A gene delivery system based on these polymers is prepared by complex coacervation of nucleic acid (DNA or RNA) with polymers. Targeting ligands and molecules that could facilitate gene transfer can be conjugated to polymers to achieve selective and enhanced gene delivery. The current invention also provides a complex composition with buffering capacity.
CN101406456A Technique for preparing florfenicol soluble powder The invention discloses florfenicol and a preparation process for compound recipe soluble powder thereof. The preparation process mainly comprises the following steps: taking 5+-0.5 grams of florfenicol, evenly mixing the florfenicol with 5-10 grams of polyethylene glycol 6000, grinding or crushing the mixture, adding oral glucose or lido powder into the mixture till the total weight reaches 100+-3 grams, screening the mixture through a No.4 sieve, packaging the mixture and obtaining the compound recipe soluble powder. The process has the advantages that: the process is simpler and quicker than an enclosing technology or a fusion eutectic technology and also has cost lower than that of the enclosing technology or the fusion eutectic technology.
WO2009145716A1 New pharmaceutical formulation useful in gerd therapy The present invention is directed to a pharmaceutical formulation comprising 3-Amino-2-f luoropropyl phosphinic acid or an enantiomer thereof, or a pharmaceutically and pharmacologically acceptable salt thereof, and its use for reducing paraesthesia in the treatment of GERD by administration of said compound.
CN101322845A Erianin inclusion compound The invention relates to an erianin product and aims at providing a product produced from the inclusion to erianin by using hydroxypropyl-Beta-cyclodextrin and series derived products of an erianin inclusion compound. The erianin inclusion compound comprises active ingredients of erianin and an inclusion agent which is hydroxypropyl-Beta-cyclodextrin and the weight ratio of the erianin to the inclusion agent is 1:8 to 1:11. Since the active ingredients of the erianin are externally wrapped with hydroxypropyl-Beta-cyclodextrin groups which have the characteristic of water solubility, the application methods of the erianin which is slightly water-soluble originally are greatly expanded. The included erianin can be prepared into tablets, capsules, oral solution, granules, injecta, etc., and can be conveniently utilized in various ways and is also easy to be absorbed by human bodies.
CN1723960A Compounding medicine for treating oral diseases, and its prepn. method A medicine for treating periodontal disease, periodontitis, periodontal atrophy, foul breath, etc is prepared proportionally from zinc oxide, rosin powder, thyme, anhydrous zinc sulfate, iodophenol powder, and calcium hydroxide through proportional mixing, stirring and loading it in bottles.
US20100226980 Novel tablet based on s-adenosyl-methionine A subject of the invention is a tablet for pharmaceutical use, particularly for veterinary use, particularly suitable for the chronic treatment of hepatic insufficiency, comprising at least one S-Adenosyl-Methionine salt. Said tablet has the advantage of being divisible and being capable of including an appetizing agent.
CN101991676A Liniment for treating vitligo and preparation method thereof The invention relates to a medicament for treating vitligo and a preparation method thereof. The medicament for treating vitligo is mainly prepared from dark plum fruit, 95% alcohol and dromisol. The preparation method comprises the steps of: soaking 40g of dark plum fruit in 100 ml of 95% alcohol, filtering after two weeks and adding 5 ml of dromisol, uniformly stirring and sealing. The medicament has good treatment effect and low price, can suit the crowds and can particularly suit people living a poor life in rural villages far from towns because of low family incomes.
US8334321 Prostaglandin fat emulsion, method for producing the same, method for stabilizing the same, and emulsifying agent A fat emulsion comprises a prostaglandin as an active ingredient, the fat emulsion comprising a phospholipid that comprises phosphatidylcholine (PC) and phosphatidylglycerol (PG) and has a ratio of PC to PG (PC:PG) of 85:15 to 99.7:0.3.
US20120115811 Phenylanaline amide derivatives useful for treating insulin-related diseases and conditions Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.
CN103044500A Preparation for organic acid and application for antibacterium The invention discloses a novel preparation method for organic acid which is separated from the cyatheaceae cyathea plant Alsophila spinutosa and the application of organic acid in the antibacterial agent. The preparation method comprises the following steps: taking the stem of the cyatheaceae cyathea plant Alsophila spinutosa as raw material, using alcohol to extract and concentrate the stem to be non-alcoholic, using chloroform to extract to remove lipid-soluble pigment and the like, then using n-butyl alcohol to extract, and separating the n-butyl alcohol extract through a chromatographic process and identifying the novel organic acid 3-acety1-4-O-Beta-D-glucopyranosidecaffeic acid. The pharmacology experiment proves that the new compound has certain antibacterial activity to various bacteria.
US20110237590 Pyridine-3-carboxyamide derivative To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1): or its salt or a solvate thereof.
CN102772601A External medicine for treating facial paralysis and preparation method thereof The invention discloses an external medicine for treating facial paralysis and a preparation method thereof. The external medicine is mainly prepared from notopterygium root, radix peucedani, bombyx batryticatus, mint, radix clematidis, folium artemisiae argyi and the like according to certain weight proportions. The medicine disclosed by the invention has the functions of dispersing wind and dispelling pathogen, dredging channels and activating collaterals and removing toxicity, is used for treating facial paralysis, takes an effect quickly, and has a good curative effect and a high cure rate.
EP2356120A1 Imidazo[1,5]naphthyridine compounds, their pharmaceutical use and compositions The present invention is directed to compounds of Formula (I), and to salts thereof, their synthesis, and their use as PI3-Kα inhibitors and/or PI3- Kα/mTOR dual inhibitors.
US7524839 Such as 1-phenylsulfonyl-4-piperazinylindole hydrochloride for treatment or prophylaxis of disease mediated by serotonin related receptor, obesity, and/or central nervous system disorder The invention-provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.
CN1883500A Application of low molecular weight citrus pectin in increasing immunity The present invention relates to a novel application of low molecular weight citrus pectin, particularly to its application in pharmaceutics, food and healthcare products. The low molecular weight citrus pectin has apparently smaller molecular weight than natural pectin and its molecular structure is improved for the reduce of methyl which makes it easy to be absorbed by intestinal canal and enter blood circulation. The citrus pectin can apparently improve appetite, strengthen immunity function, modulate immunity turbulence, reduce cholesterol and prevent atherosclerosis. After entering into the blood circulation, it can help people get rid of poisonous heavy metals. Therefore, the low molecular weight citrus pectin is used to prepare medicine, food and healthcare products, which can reinforce immunity functions.
US20100099638 Immunocompetent xenograft model The teachings are directed to an immunocompetent xenograft model. The model comprises an immunodeficient animal modified to have a reconstituted immune system, wherein a xenograft is transplanted in the animal and allowed to establish for an establishment period of at least about 10 days. The xenograft simulates a tissue in a subject in need of a treatment. In these embodiments, the reconstituted immune system is created after the establishment period, and is created by administering a total number of T-cells to the animal. The total number of T-cells consists of a preselected number of responsive T-cells, a preselected number of non-responsive T-cells, and a preselected ratio of responsive T-cells to total T-cells. The preselected number of responsive T-cells simulates a number of responsive T-cells in the subject, and the ratio of the number of responsive T-cells to total T-cells ranges from about 1:100,000 to about 30:100,000.
US20090215787 Preparations of new polymorphic forms of varenicline tartrate The present invention is directed to an amorphous form, three novel polymorph form of crystalline varenicline tartrate, namely Form D, Form E and Form F. The present invention also provides processes of their preparations and pharmaceutical composition comprising such material and their use in therapy. Form D is new anhydrous varenicline tartrate, and can be prepared from recrystallizing varenicline tartrate in a mixture of methanol and water or a mixture of N,N-dimethylformamide and water. Form E is a new varenicline tartrate monohydrate, and can be prepared recrystallizing varenicline tartrate in a mixture of isopropanol and water. Form F is another new varenicline tartrate monohydrate, and can be prepared recrystallizing varenicline tartrate in a mixture of acetone and water. The X-ray powder diffraction pattern (X-RPD), Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) techniques are used to characterize amorphous form and crystalline polymorphic forms.
WO2013023511A1 Triazolopyrimidine derivative and preparation method and use thereof The present invention relates to triazolopyrimidine derivatives and a preparation method and a use thereof. In particular, the present invention relates to triazolopyrimidine derivatives as shown in general formula (I), and the use thereof as a therapeutic agent, especially as a P2Y12 receptor antagonist, wherein the definition of each substituent in general formula (I) is the same as the definition in the description.
US20110177158 Liposomes Capable of Effectively Binding the Beta Amyloid Peptide Novel liposomes are described which are capable of effectively binding beta amyloid peptide and are useful for the treatment, prevention and diagnosis of Alzheimer's disease. Binding ability is provided by the presence in the formulation of particular natural lipids identified by the Applicant. These comprise a constant component, made up of cholesterol and sphingomyelin, and an additional variable component, made up of selected lipids.
US20070249620 Urea Derivative The present invention relates to a urea derivative or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect. A urea derivative having the formula: [wherein R1 is a C6-C10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; R is a C6-C10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; E is a group having the formula (II) or the formula (III) (wherein R3 is a hydrogen atom or others; R4 and R5, which are the same or different, are a hydrogen atom or others; X and U, which are the same or different, are a group represented by the formula CH or others; m and n, which are the same or different, are I or another number) or others; and A is a group represented by the formula —NH—C(═O)— or others], or a pharmacologically acceptable salt thereof.
WO2005092320A1 Cytoprotective composition A cytoprotective composition which comprises a formylated phenyl or pyrrole compound represented by any of the following formulae (I) to (IV) and a carrier: Wherein R1 is H, OR3, OR4, NHR3, NHR4, SR3, SR4, SO3R3, SO3R4, (CH2)nR3, (CH2)nR4, (CH=CH)nR3, (CH=CH)nR4, C(=O)R3, C(=O)R4, PhR3, PhR4, or (CH2)nCHR3R4; R2 is any of the groups defined for R1 or C(NHR3)R3; R3 is substituted or unsubstituted straight-chain C1-6 alkyl; R4 is carboxylated straight-chain C1-6 alkyl; and n is an integer of 0 to 6.
EP1250133B1 Ophthalmic anti-allergy compositions suitable for use with contact lenses Topically administrable anti-allergy compositions comprising olopatadine and a polymeric quaternary ammonium preservative are suitable for use by patients wearing contact lenses.
CN1806801A Pharmaceutical composition of sodium houttuyfonate for treating respiratory infection and preparation method thereof The invention relates to a sodium new houttuyfonate pharmaceutical composition for treating respiratory tract infection and process for preparation, wherein the pharmaceutical composition comprises sodium new houttuyninum, Poloxamer or Tween-80, the preparing process comprises dissolving Poloxamer or Tween-80 into water, charging sodium hydrogen sulfite to adjust PH to 1.5-8.5, charging sodium new houttuyninum, mixing and charging excipient, isotonic agent. The dosages types include small liquid drug injections, freeze-dried powder injections, asepsis split charged powder injections, high capacity injections or fluid infusions.
CN103623345A Preparation method of antivirus oral liquid The invention discloses a preparation method of antivirus oral liquid. The preparation method comprises the following steps: firstly crushing reed rhizome, radix rehmanniae, radix curcumae, rhizoma acori graminei, radix isatidis, pogostemon cablin, rhizoma anemarrhenae, forsythia and gypsum, uniformly mixing, extracting by using a water vapor distillation method, separating so as to obtain volatile oil and an extracting solution; concentrating the extracting solution, dehydrating the volatile oil, dissolving and treating the dehydrated volatile oil, phospholipid and cholesterol in a solvent so as to obtain a volatile oil liposome solution; adding auxiliary materials to the concentrated solution, adjusting the pH value, then adding the volatile oil liposome solution to the concentrated solution for fixing the volume, filtering so as to obtain the antivirus oral liquid, finally filling and sterilizing. According to the preparation method, liposome is used for encapsulating the volatile oil, so that the encapsulation efficiency is relatively high, and the encapsulation rate can reach about 95%. The preparation method is used for preparing the antivirus oral liquid and can be used for obviously improving the stability of the volatile oil and ensuring the curative effect of a product.
CN1745751A Preparation composition for eyes An ocular medicine in the form of gel is prepared from epinastine hydrochloride, EDTA, carbomer, alkali and purified water through dissolving EDTA in purified water, adding others, high-speed stirring, and adding alkali for neutralizing. Its advantages are easy absorption and high biologic utilization rate.
US7276593 Proteins and nucleic acids encoding same Disclosed are polypeptides and nucleic acids encoding same. Also disclosed are vectors, host cells, antibodies and recombinant methods for producing the polypeptides and polynucleotides, as well as methods for using same.
CN103520102A Vitamin D nano-emulsion and preparation method thereof The invention provides a vitamin D nano-emulsion and a preparation method thereof. The vitamin D nano-emulsion comprises vitamin D and tween-80 in a mass ratio of 1:(1-6), and water of which the mass is 0.8-4.5 times of the total mass of vitamin D and tween-80. The method comprises the following steps: adding vitamin D and tween-80 into a container, uniformly mixing, and adding water to obtain a mixed solution; performing ultrasonic treatment on the mixed solution until the mixed solution is clear and transparent to obtain the vitamin D nano-emulsion. The method is used for preparing the vitamin D nano-emulsion by adopting an ultrasonic emulsification method, is simple in production process, mild in condition, short in preparation time and low in equipment requirement. The prepared vitamin D nano-emulsion is of an oil-in-water mode, is clear and transparent, good in water solution and good in stability, has a grain distribution range of 28-66nm and average grain diameter of 41nm, and accords with the basic characteristics of a nano-grade material.
CN102448496A Medicine composition having iodine and steroid and application to treatment of rhinitis The invention provides a medicine composition comprising iodine and steroid and introduces the uses of the medicine composition in treating respiratory tract diseases and the method of using the medicine composition.
US20140066440 Highly Concentrated Stable Meloxicam Solutions for Needleless Injection A method for treating pain, inflammation, fever and respiratory complaints in mammals comprising administering by needleless injection to a mammal in need of such treatment an aqueous cyclodextrin-free solution of meloxicam containing a pharmacologically acceptable meloxicam salt of an organic or inorganic base.
US20100215769 Natural occurring nutrient supplement compositions and methods of treatment using same by improving resistance to DNA damage, enhancing DNA repair and stimulating immune function wherein metabolic competition is avoided Selectively administering to humans, as a daily dosage, a combination of resveratrol-carotenoids, nicotinamide (or niacin or a precursor thereof) and a source of zinc, in excess of normal dietary levels, for improving resistance to DNA damage, enhancing DNA repair capacity, and stimulating immune function.
US20100279979 Immunopotentiating agent for use in animals A simplified method for producing an immunopotentiating agent from cell walls of yeast, other fungi or bacteria is provided and its use as an additive to animal feed to increase resistance to various infections and to potentiate the effect of vaccines is described.
CN103040738A Drug composition containing hydroxyfasudil compound The invention provides a drug composition containing a hydroxyfasudil compound, which comprises hydroxyfasudil, sodium dihydrogen phosphate, dextran 40, methionine and water for injection. A preparation method of the drug composition comprises the following steps of stirring and dissolving sodium dihydrogen phosphate, methionine, hydroxyfasudil and dextran with the water for the injection, adding active carbon for decoloration, filtering removing carbon, and then conducting filter sterilization and autoclaved sterilization. The drug composition containing hydroxyfasudil is simple in prescription and reduces the possibility of hypotension, the stability is improved by reasonable configuration, and application and popularization of a hydroxyfasudil injection is facilitated.
CN101843613B Vitamin EC chewable tablets with high stability and preparation method thereof The invention discloses vitamin EC chewable tablets with high stability and a preparation method thereof and belongs to the field of pharmaceutics. The chewable tablets comprise vitamin E, vitamin C, a filler, an adhesive, a fluidizer, a stabilizing agent and a flavoring agent. In the process of preparing the chewable tablets, powder coating technology is adopted to coat the vitamin C, so the prepared chewable tablets have high stability and high safety and are convenient to transport and store.
CN102120034A Novel targeted medicament targeted to brown adipose tissues for treating obesity The invention relates to the technical field of biomedicine, in particular to a novel targeted medicament targeted to brown adipose tissues for treating obesity. According to the novel targeted medicament targeted to the brown adipose tissues for treating obesity, the medicament is formed by connecting brown adipose tissue-targeted polypeptide CKGGRAKDC-NH2 and an 11beta hydroxysteroid dehydrogenase 1 inhibitor, acts on the brown adipose tissues in a targeted way, amplifies the function of brown adipose, and has no affinity or actions on other visceral organs, so that the purpose of treating the obesity more efficiently is achieved.
EP1750724A1 Method for improving cognitive function by co-administration of a gabab receptor antagonist and an acetylcholinesterase inhibitor The present invention provides methods and compositions for improving cognitive function by administering a GABAB receptor antagonist and an acetylcholinesterase inhibitor.
WO2008093919A1 Use of n-benzyl-n-(2-dimethylamino-ethyl)benzenesulfonamide derivatives for treating central nervous system disorders The present invention relates to N-benzyl-N-(2-dimethylamino-ethyl)-benzenesulfonamide compounds useful for the treatment of central nervous system (CNS) disorders.
US20090036519 Peroxisome proliferator activated receptor ligand and process for producing the same The present invention easily and efficiently provides a peroxisome proliferator-activated receptor ligand, and a composition for amelioration of insulin resistance or for prevention and/or amelioration of the insulin resistance syndrome containing the same, as an active ingredient. The present invention relates to a peroxisome proliferator-activated receptor ligand which comprises a prenylflavonoid, a chalcone derivative exclusive of prenylflavonoids, a flavonol derivative exclusive of prenylflavonoids, and a salt, a glycoside and/or an esterified substance thereof acceptable as a pharmaceutical preparation or a food or a beverage; a composition containing the above ligand; a plant-derived extract containing the above ligand; and a process for producing the above extract.
CN103550242A Pharmaceutical composition for treating hepatic fibrosis and preparation method thereof The invention relates to a pharmaceutical composition for treating hepatic fibrosis and a preparation method thereof. The pharmaceutical composition is a formulation prepared from a main ingredient and pharmaceutically acceptable auxiliary materials, wherein the main ingredient comprises 100-300 parts of pirfenidone and 50-150 parts of inosine. The formulation of pirfenidone and inosine is stable in quality, controllable, safe and effective. In clinic, the formulation is mainly used for the treatment of diseases of hepatic fibrosis, cirrhosis, liver cancer, and the like.
EP2331529A2 Novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone and pharmaceutical compositions thereof Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.
CA2227533C Improved therapeutic agents This invention relates to now nucleoside derivatives of formula (I); wherein R1 and R2 are independently selected from hydrogen, elaidoyl, oleoyl, stearoyl, eicosenoyl (cis or trans) and eicosanoyl, with the provisos that R1 and R2 cannot both be hydrogen, oleoyl or stearoyl, R1 cannot be hydrogen when R2 is oleoyl or stearoyl, and R2 cannot be hydrogen when R1 is elaidoyl, oleoyl or stearoyl. Further, the invention relates to the use of the nucleoside derivatives of formula (I) wehrein R1 and R2 are independently selected from hydrogen, and C18- and C20-saturated and mono-unsaturated acyl groups, with the provisos that R1 and R2 cannot both be hydrogen, in the manufacture of a pharmaceutical preparation for the treatment of tumours.
CN103267852A Application of fibroblast activation protein (FAP) alpha to preparation of pancreatic cancer prognosis kit The invention relates to an application of fibroblast activation protein (FAP) alpha to the preparation of a pancreatic cancer prognosis kit and an application of an FAP alpha inhibitor to the preparation of drugs for treating pancreatic cancer. The high expression of the FAP alpha in pancreatic cancer tissue mesenchyme of a testee has shorter overall survival than low expression. The FAP alpha inhibitor can be used for inhibiting the effects of FAP alpha (+) pancreatic stellate cells on promoting the pancreatic cancer migration, invasion and metastasis in vivo, which hints that the FAP alpha inhibitor can be used for inhibiting the metastasis of the pancreatic cancer and decelerating the progress of pancreatic cancer; and aiming at the pancreatic cancer mesenchyme treating strategy, the comprehensive treatment effect for the pancreatic cancer is possibly improved.
CN102836158A Lipid body loaded with chloroquine drugs and paclitaxel drugs together and preparation method of same The invention discloses a lipid body loaded with chloroquine drugs and paclitaxel drugs together. The lipid body comprises drugs, phosphatide, cholesterin compounds, an internal buffering system and pH value conditioning agents, wherein, the mass ratio of the drugs, the phosphatide and the cholesterin compounds is 1:2 to 125:1 to 45; and the drugs are the chloroquine drugs and the paclitaxel drugs. Due to the chloroquine drugs and the paclitaxel drugs, the lipid body loaded with chloroquine drugs and the paclitaxel drugs together is characterized in that multidrug resistance can be inhibited, and the drug toxicity can be reduced. The invention further discloses a preparation method of the lipid body loaded with chloroquine drugs and the paclitaxel drugs together; in addition, the preparation technology is simple, the condition is mild, controlling parameters are less, and the preparation method facilitates to lower the manufacturing cost and achieves easy industrialized production.
US20120010161 Novel azapeptide or azapeptidomimetic compounds inhibiting bcrp and/or p-gp The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.
US7666398 Polyanhydride linkers for production of drug polymers and drug polymer compositions produced thereby Polyanhydrides which link low molecular weight drugs containing a carboxylic acid group and an amine, thiol, alcohol or phenol group within their structure into polymeric drug delivery systems are provided. Also provided are methods of producing polymeric drug delivery systems via these polyanhydride linkers as well as methods of administering low molecular weight drugs to a host via the polymeric drug delivery systems.
CN1814047A Chinese remedy medicinal dry-mixed suspension preparation for treating common cold and preparing method The invention discloses a Zhongganling dry-mixing suspension having efficacies of inducing sweat and clearing heat and the preparing method thereof, and it is prepared of Chinese and West medicinal raw materials and auxiliaries in weight proportion: root of kudzuvine 1700í½2700g, Artemisia apiacea 300í½900g, Pubescent holly root 1500í½2700g, notopterygium root 100í½400g, verbena 1000í½2000g, plaster 150í½450g, banlangen 600í½1800g, analgin 100í½300g, chlorphenamine maleate 1í½4g, mannitol 100í½300g, hypromellose 70í½270g, aspartame 20í½80g, orange powder 5í½80g, sodium glutamate 5í½50g, carboxyl methyl starch sodium (CMS-Na) 10í½80g, by crushing, screening, weighing and mixing, decocting, filtering, concentrating, drying and making particles and split-charging into 1000 bags; the invention has characters of fast absorptivity, high curative effect, convenience for taking and carrying, and especially has very good curative effect on influenza.
CN1593658A Coupled compound of 3-amino-2-oxazolidinone and preparation method thereof The invention discloses a 3-amino-2-oxazolidinone (AOZ) coupling substance with a general formula (I), which is composed by optimizing cow serum protein from 3-amino-2-oxazolidinone haptene and carrying agent substance for producing immunogen performance, wherein n is the number of molecules of AOZ combining with a cow serum protein, BSA is cow serum protein, its molecular weight range is between 6.6KDa-6.9KDa. The invention also discloses the process for preparing the coupling substance.
US20110305709 Calcium sensor stim1 and the platelet soc channel orai1 (cracm1) are essential for pathological thrombus formation The present invention relates to a pharmaceutical composition comprising an inhibitor of stromal interaction molecule 1 (STIM1) or an inhibitor of STIM1-regulated plasma membrane calcium channel activity, in particular an inhibitor of Orai1 (also designated as CRACM1), and optionally a pharmaceutically active carrier, excipient or diluent. The invention further relates to an inhibitor of stromal interaction molecule 1 (STIM1) or an inhibitor of STIM1-regulated plasma membrane calcium channel activity, in particular an inhibitor of Orai1 (also designated as CRACM1), for treating and/or preventing a disorder related to venous or arterial thrombus formation.
US7276525 Administering either simultaneously or sequentially a bone morphogenic protein and a compound having a transforming growth factor-beta selective inhibitory activity, particularly 4-(4-benzo[1,3]dioxol-5-yl-5-pyridin-2-yl-1H-imidazol-2-yl)benzamide It is an object of the present invention to provide an excellent enhancer for an osteogenesis accelerator that can enhance the activity of BMP as an osteogenesis accelerator. Another object of the present invention is to provide a method of screening for a novel enhancer for an osteogenesis accelerator. The present invention relates to an enhancer for an osteogenesis accelerator, which comprises a compound having a TGF-β selective inhibitory activity as an active ingredient, the enhancer being administered with an osteogenesis accelerator containing BMP as an active ingredient either simultaneously or sequentially, and to a method of screening for an enhancer for an osteogenesis accelerator, comprising using a TGF-β inhibition as a measure for discovering the enhancer.
US20110105622 Pharmaceutical composition containing glur2-lacking ampar antagonist for preventing or treating psychiatric illnesses A pharmaceutical composition, comprising a GluR2-lacking AMPAR antagonist as an active ingredient, is effective for preventing or treating mental diseases selected from the group consisting of posttraumatic stress disorder (PTSD), drug addiction, and phobia.
CN101972227A Method for preparing erianin self-emulsifying preparation The invention discloses a method for preparing an erianin self-emulsifying preparation. The preparation comprises the following components in part by weight: 0.5 to 5 parts of erianin, 35 to 60 parts of oil, 20 to 60 parts of emulsifier and 5 to 20 parts of auxiliary emulsifier. The method comprises the following steps of: adding the erianin serving as a raw material into a self-emulsifying substrate; protecting by using N2; performing ultrasonic oscillation at the temperature of 30 to 75 DEG C to obtain the erianin self-emulsifying preparation; cooling to room temperature; adding a medicinal auxiliary material; and preparing into the preparation formulations such as tablets, dripping pills, capsules, soft capsules and the like by a conventional method. The preparation of the invention has high bioavailability, high self-emusifying capacity and low taking dosage, and is convenient to use.
CN1875945A Lyophilized powder injection of cepharantine hydrochloride and preparation method thereof The invention discloses a freeze dried stephanine hydrochloride injection for treating leukopenia caused by radiotheraphy and chemotherapy, which comprises the following medicaments (by weight ratio): stephanine hydrochloride 1-10 parts, freeze-drying excipient 10-400 parts. The invention also discloses the process for preparing the freeze dried injection. The freeze-drying excipient can be mannitol, glucose, trehalose, sucrose or lactose.
US20120058173 Selective starch feeding protocol The present invention includes a method for improving milk production in a ruminant. An amount of ruminally digestible starch in relation to the dry matter of a feed is manipulated to include a first selected ratio of ruminally digestible starch in relation to the dry matter of the feed which is fed to the ruminant during a first time interval after parturition. After the first time interval, the amount of ruminally digestible starch component in the dry matter of the feed is adjusted to a second ratio, lower than the first ratio, and fed to the ruminant.
CN101244168A Externally used liquid for treating burn and scald The invention discloses an external therapy liquid medicine for treating burn and scald. The medicine is made of gotu kola bark, luderick grass root, yellow bubble tree bark, hairy dog leaf bark, wild kiwi fruit root, camphor tree root and distilled spirit which are mixed according to a certain proportion. The preparation method comprises the following steps: wash, crush respectively and mix gotu kola bark, luderick grass root, yellow bubble tree bark, hairy dog leaf bark, wild kiwi fruit root and camphor tree root to pour into a vessel; infuse the distilled spirit; ignite the distilled spirit and burn to the composition when the distilled spirit leaves 30 percent; and use a gauge to filter the residue of the composition. The external therapy liquid medicine has the advantages that the external therapy liquid medicine overcomes the deficiency of the prior art and provides a therapy liquid without pollution which uses a wild plant on the high mountain as the material; the cost is low because the material comes from the nature; the medicine has no grease so as to make the skin easily absorb; the pain can be taken away within a plurality of minutes; and the skin repairs quickly without scar.
US7375135 Fatty acid derivatives; preparation and uses thereof The invention concerns novel molecules, their preparation and their uses, in particular in the field of human and veterinary medicine and cosmetics. The inventive compounds are partly fatty acid derivatives and exhibit advantageous pharmacological and cosmetic properties. The invention also concerns various uses of said compounds, the pharmaceutical compositions containing them and methods for preparing them. The inventive compounds are useful in particular for preventing and/or treating dyslipidemiae, cardiovascular diseases, syndrome X, restenosis, diabetes, obesity, hypertension, certain cancers, dermatological diseases and in cosmetics, for fighting against skin aging and its effects notably against wrinkles and the like.
WO2006092579A1 Microcrystalline ( 5-fluoro-2-methyl-3-quinolin-2-ylmethyl-indol-1-yl) acetic acid The invention relates to a microcrystalline form of a compound which is an inhibitor of PGD2 at the CRTH2 receptor. The microcrystalline form is obtained from a simple chemical reaction without the need for a milling process.
EP1551815A1 Thiazole compounds for the treatment of neurodegenerative disorders The invention provides compounds of Formula (I): wherein R1, R2, R3, R4, R6, R7, and A are as defined. Compounds of Formula (I) have activity inhibiting production of Aß-peptide. The invention also provides pharmaceutical compositions and methods for treating diseases, for example Alzheimer's disease, in mammals comprising compounds of Formula (I).
WO2011149471A1 Method to prevent/treat post-operative induced constipation A method of treating post-operative induced constipation in a patient includes the steps of (a) providing a solution comprised of glucose 50% in sterile IV solution; (b) adding a predefined amount of regular insulin to the solution; (c) adding a predefined amount of potassium to the solution, wherein the predefined amount of potassium is based on the serum potassium level of the patient; (d) administering the solution into the patient at a predefined infusion rate; (e) monitoring the electrolyte level of the patient at a predetermined time after administration of the solution; and (f) decreasing the infusion rate based upon determined bowel movement in the patient.
CN102552146A Epirubicin liposome as well as preparation method and preserving method thereof The invention belongs to the field of pharmaceutical preparation and relates to an epirubicin liposome as well as a preparation method and a preserving method of the epirubicin liposome. The epirubicin liposome is formed by epirubicin and at least one phospholipid as, well as at least one surface active agent or one cryoprotectant or cholesterol which may be contained. The preserving method comprises the following types: preservation at normal temperature, refrigeration preservation, freezing preservation and freezing and drying preservation.
US20130284168 Drug Delivery System And Method For Conscious Sedation/Analgesia Inhalant anesthetics are developed with a number of properties including rapid onset and recovery, controllability, and, ideally, a broad safety profile. The efficacy of these agents is measured by their ability to create anesthesia within the framework of the other desirable properties. The instant invention focuses on the dosage level where analgesia occurs but amnesia or lack of consciousness does not. In addition to identifying the dosage level where pain is sharply reduced or eliminated but awareness remains, a delivery system for safe and effective delivery of the agent is described.
EP2178868A1 Bicyclic heteroaryl compounds and their use as kinase inhibitors Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.
CN101953844A Medicament for improving sperm quality and treating male sterility The invention discloses a medicament for improving sperm quality and treating male sterility. The medicament consists of the following components: L-carnitine, arginine, vitamin E, nucleotide, zinc gluconate, clomiphene, sodium selenite and vitamin A, wherein the ratio of the L-carnitine to the arginine to the vitamin E to the nucleotide to the zinc gluconate to the clomiphene to the sodium selenite and to the vitamin A ranges from 140:140:7:7:7:3.5:1:1 to 80:80:4:4:4:2:1:1. A method for preparing the medicament for improving the sperm quality and treating the male sterility comprises the following steps of: (1) selecting qualified raw materials of each component of the medicament according to the ratio and uniformly mixing; (2) adding excipient auxiliary materials and uniformly mixing again; and (3) drying to prepare an oral preparation. The medicament has the advantages of obvious curative effect of improving the sperm quality and treating the male sterility, convenient administration, synergistic effect of components, and capacities of reducing toxic or side effect and improving the curative effect.
US7078394 dominant estrogenic activity phase of three daily doses of an estrogen equivalent to 1 mg per day of 17 beta -estradiol per day and a dominant progestagenic activity phase of a combination of an estrogen as above and a progestogen equivalent to 90 mu g per day of norgestimate. A hormone replacement therapy, comprising a plurality of daily doses of a pharmaceutical preparation, the doses being administered continuously and consecutively in alternating phases of three daily doses, a relatively dominant estrogenic activity phase comprising three daily doses of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17β-estradiol per day, and a relatively dominant progestagenic activity phase of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg per day of norgestimate.
WO2010098482A1 Stable capsule preparation and method for producing same Disclosed is a capsule preparation containing pitavastatin and fenofibrate as active ingredients. The capsule preparation containing pitavastatin and fenofibrate is produced by filling a composition prepared by mixing magnesium oxide and/or magnesium hydroxide with the active ingredients in a capsule. The capsule preparation is stable over time.
US20050220905 Tribulus terrestris, Turnera diffusa and Cinnamon cassia extracts in a precise weight ratio with Ginkgo biloba extract and a carrier or excipient; impotence, erectile dysfunction; reduced libido; frigidity; anorgasmia; side effect reduction; vasodilation; dopaminergic agents; phosphodiesterase inhibitor Disclosed are pharmaceutical compositions containing: extracts of Tribulus terrestris, Turnera diffusa and Cinnamon cassia in tile weight ratio of 1.5-3.5:1-2:0.1-0.4 respectively; Ginkgo biloba extract, and optionally arginine or a physiologically equivalent esters salts or precursor thereof. The compositions according to the invention are useful in the treatment of male and female sexual dysfunctions.
WO2010094821A1 Use of vaginally-administered insulin sensitizing agents The invention relates to the use of vaginally-administered insulin-sensitizing agents for preventing and/or treating hyperandrogenism and/or polycystic ovarian syndrome and/or related disorders.
WO2011024077A3 Exon skipping therapy for functional amelioration of semi functional dystrophin in becker and duchenne muscular dystrophy Methods for stabilizing unstable proteins or for restoring functionality to non-functional or poorly functioning (semi-functional) proteins using exon skipping technology are provided. The methods involve the administration of antisense oligonucleotides to cause exon skipping, thereby removing one or more exons responsible for protein instability or lack of functionality. For example, exons encoding protease recognition sites may be removed. The method is useful for treating diseases caused by protein instability, such as Becker Muscular Dystrophy, or for treating Duchenne Muscular Distrophy patients with semi-functional dystrophin due to treatment with other exon skipping or stop codon readthrough therapies.
US8124616 Bicyclic PPAT inhibitors as antibacterial agents Disclosed are compounds of Formula I, pharmaceutical compositions comprising Formula I and methods of treating bacterial infections. The disclosed compounds are inhibitors of PPAT (phosphopantetheine adenyl transferase), and are useful in the treatment and prevention of diseases caused by bacteria, particularly bacteria dependent on PPAT, for example, species such Escherichia coli, Helicobacter pylori, Staphyloccocus aureus, and the like.
US20060079545 Palonosetron for the treatment of chemotherapy induced emeses Methods and compositions for reducing chemotherapy and radiotherapy induced emises with 5-HT3 receptor antagonists are disclosed, especially with palonosetron.
WO2007086584A1 NOVEL INHIBITOR OF FabK AND FabI/K Disclosed is a compound which can inhibit both of FabI and FabK which are fatty acid synthases to show a wide antibacterial spectrum including Streptococcus pneumoniae, Pseudomonas aeruginosa and Enterococcus faecalis, and therefore can be used for the treatment of a bacterial infection.
US20110288180 Dietary purgatives Described are kits, food compositions and methods for cleaning the bowel, e.g., in preparation for a medical procedure, e.g., a diagnostic or treatment procedure, such as an endoscopic or surgical procedure, or radiologic imaging such as CT colography.
US7256200 administering mixture of opioid and calmodulin kinase inhbitor Composition and methods of treating pain and reducing, reversing, or preventing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and a calcium calmodulin kinase (CaMKII) inhibitor as active agents to treat pain in mammals, including humans.
EP1511493A1 Use of peroxovanadium compounds as tumour cell growth suppressor The present invention relates to the use of peroxovanadium compounds as antitumorigenic agents. These compounds have been found to be suitable, at low dosages, as antitumorigenic agents in the treatment of cancer, such as breast cancer and prostate cancer. It has been found that even at low dosages, these compounds can prevent or arrest further tumour growth.
US20120328573 Composition for Maintaining Healthy Kidney Function The present invention provides a composition comprising prebiotic and probiotic components and is used to reduce elevated levels of nitrogenous waste products and to promote a healthy bowel microenvironment.
US20060116326 Benzothiophene compounds having antiinfective activity Benzothiophene compounds such as are DNA binding compounds exhibiting antibacterial activity.
US20130071342 Cosmetic composition comprising coumestrol or a bean extract containing coumestrol for skin care The present invention relates to a cosmetic composition for skin care, comprising coumestrol or a bean extract containing coumestrol.
CN101434627B 2'-fluoro-4'-substituted nucleoside analogue, synthetic method and use thereof The invention discloses a nucleoside analogue and a preparation method and application thereof, more particularly relates to 2'-fluorin-4'-substituted nucleoside analogue or salts thereof or 5'-phosphate ester thereof and a preparation method and application thereof. The nucleoside analogue has a general formula shown below, wherein R is CH3, CN, N3, ethynyl; X is F, OH, NH2; Y is H, CH3, F, OH, NH2. and can be applied to treat virus infections, particularly the infections of HBV, HCV or HIV, with good activity.
US20120321597 Methods and compositions for regenerating connective tissue Connective tissue regenerative compositions and methods of repairing and regenerating connective tissue using such compositions are provided. The compositions generally comprise a bioactive hydrogel matrix comprising a polypeptide, such as gelatin, and a long chain carbohydrate, such as dextran. The hydrogel matrix may further include polar amino acids, as well as additional beneficial additives. Advantageously, the compositions include further components, such as osteoinductive or osteoconductive materials, medicaments, stem or progenitor cells, and three-dimensional structural frameworks. The compositions are useful for regenerating connective tissue, and can be administered to an area having injury to, or a loss of, connective tissue, such as bone, cartilage, tendon, and ligament.
WO2007014652A1 TREATMENT OF TUMOURS WITH IKK-ß INHIBITORS The application relates to the use of an IKK-beta inhibitor through production of medicaments for treating tumours, and to medicaments comprising the said IKK-beta inhibitor.
CA2801842A1 Amorphous varenicline tartrate co-precipitates Disclosed herein is a stable amorphous coprecipitate comprising varenicline tartrate and a pharmaceutically acceptable excipient selected from the group consisting of maltodextrin, lactose monohydrate and 2-hydroxypropyl-ß-cyclodextrin, method for the preparation, pharmaceutical compositions, and method of treating thereof. Advantageously, the amorphous coprecipitates of varenicline tartrate disclosed herein have improved physiochemical characteristics that assist in the effective bioavailability.
US20100249225 C-(2-Phenyl-Cyclohexyl)-Methylamine Compounds for the Treatment of Anxiety Disorders Pharmaceutical formulations of [2-(3-methoxyphenyl)-cyclohexylmethyl]-dimethylamine and the metabolites thereof for treating anxiety, anxiety attacks and disorders as well as depression. Related methods of treating anxiety and anxiety attacks or depression are also provided, including methods of administering the active compounds as adjuvants to an antidepressant.
WO2006065555A2 Use of alpha-adrenergic blockers for the treatment of dysmenorrhea Use of an alpha-adrenergic blocker for the preparation of a medicament for treating primary dysmenorrhea in a human female suffering from the same. Exemplary alpha-adrenergic blockers are phenoxybenzamine, alfuzosin, doxazosin, terazosin, prazosin, and tamsulsoin, or a pharmaceutically acceptable salt or ester thereof. Tamsulosin HC1 is preferred.
DE102005041760A1 New fredericamycin A derivatives with carbon-bonded B-ring substituent, are well tolerated topoisomerase I and/or II inhibitors especially useful for treating cancers or tumors Fredericamycin A derivatives (I), carrying a C-bonded organic substituent in the B-ring, are new. Fredericamycin derivatives (I) of formula (Ia) or (Ib) (including stereoisomers and tautomers) and their salts and inclusion compounds are new. R1 : H, 1-6C alkyl, cycloalkyl or 1-4C alkyl-cycloalkyl; R2, R3 : 1-14C alkyl, 2-14C alkenyl, 1-4C alkylaryl, heteroaryl, 1-4C alkylheteroaryl, cycloalkyl, 1-4C alkyl-cycloalkyl, heterocycloalkyl, 1-4C alkyl-heterocycloalkyl, CHO, optionally esterified or amidated COOH or a wide range of specific substituted alkyl groups; R5, R6 : H, 1-14C alkyl, 2-14C alkenyl, aryl, 1-4C alkylaryl, heteroaryl, 1-4C alkylheteroaryl, cycloalkyl, 1-4C alkyl-cycloalkyl, heterocycloalkyl, 1-4C alkyl-heterocycloalkyl or various specific substituted alkyl groups; or together complete a 5-7 membered ring; R4, R7, R8 : H, 1-6C alkyl or a wide range of specific substituted carbonyl groups; X1, X2O, S, NH, N(1-8C alkyl) or N(cycloalkyl); Y1, Y2O or N(R5); and X2-R6 can be replaced by H if Y1 or Y2 = NR5; Y3O, S or NH. [Image] - ACTIVITY : Cytostatic; Dermatological; Antiinflammatory; Antiparasitic; Immunosuppressive. - MECHANISM OF ACTION : Topoisomerase I and/or II inhibitor.
US20100016266 Pyridine Imidazoles and Aza-indoles as Progesterone Receptor Modulators The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.
US20090182022 Treatment of Fatty Liver Methods and compositions comprising peroxisomal and/or mitochondrial beta oxidation stimulating agents to reverse or resolve, slow the progression of, treat or prevent the development of fatty liver and conditions stemming from fatty liver, such as NASH, liver inflammation, cirrhosis and liver failure. An active agent that by itself is associated with an increased risk of fatty liver development and conditions stemming from fatty liver, such as NASH, liver inflammation, cirrhosis and liver failure, may be administered in combination with peroxisomal and/or mitochondrial beta oxidation stimulating agents. A combination regimen involving such agents, as simultaneous or concomitant therapy, or as a fixed dosage form, is also provided.
WO2011014588A2 Dermal formulations of dp2 receptor antagonists Described herein are topical formulations for use in the treatment or prevention of dermatological diseases, disorders, or conditions in a mammal. Topical formulations disclosed herein include a DP2 receptor antagonist compound formulated for dermal administration
US20120231057 Treatment and prevention of dental pathology in humans and non-human animals The present invention relates to methods and compositions for inhibiting, treating, and preventing dental diseases in human and non-human animals, particularly domesticated companion animals. More particularly, the present invention relates to the unexpected discovery that the combination of micron-sized particulate bioactive glass and a topical bisphosphonate yields a composition that is capable of treating and/or preventing dental problems such as periodontal disease, tooth decay and tooth resorption in animals, particularly small mammals such as cats.
US20100324110 Self Solidifying Bioerodible Barrier Implant Provided are bioerodible compositions that can be implanted into cavities of mammalian tissue as a liquid or semi-liquid and which solidify upon exposure to body temperature of the mammal. The implants erode over a prescribed period of time and elute a drug. The implants also form a seal with the skin or mucosa surrounding the cavity to prevent the entry of bacterial pathogens.
US20100168085 Dopamine and agonists and antagonists thereof for modulation of suppressive activity of CD4+CD25+ regulatory T cells Compositions and methods for modulation of the suppressive activity of CD4+CD25+regulatory T cells (Treg) on CD4+CD25− effector T cells (Teff) are provided. An agent selected from: (i) dopamine; (ii) a dopamine precursor; (iii) a D1-R agonist; (iv) a D2-R antagonist; (v) a combination of (i) and (ii); or (vi) a combination of (i), (ii) or (iii) with (iv), down-regulates the suppressive activity of Treg and is useful for treatment of cancer. An agent selected from (i) a dopamine D2-R agonist, (ii) a dopamine D1-R antagonist, and (iii) a combination of (i) and (ii), up-regulates the suppressive activity of Treg and is useful for treatment of an autoimmune disease or for controlling graft rejection in tissue/organ transplantation.
US20070037870 Novel substance having alpha-glucosidase inhibiting activity and food containing the same To provide a novel substance having α-glucosidase inhibiting activity, derived from natural products and being safe, which substance has not only a blood sugar ameliorating activity being effective in the prevention or treatment of diabetes or obesity but also an activity of reducing postprandial hyper-blood sugar, etc. and to provide food containing the same. [MEANS FOR SOLVING PROBLEMS] A substance having α-glucosidase inhibiting activity, represented by the formula:
CN101143210A Compound fatty milk oral preparation An oral preparation of compound fat emulsion belongs to a nutritious product which is confected by a prescription. The raw material includes midchain fatty acid glyceride (MCT), calcium caseinate/sodium peptide caseinate, refined egg yolk lecithin, pharmaceutical glycerin and purified water. The prescription is 10 to 200 g of the MCT, 0 to 30 g of the calcium caseinate or the sodium peptide caseinate, 0 to 30 g of the refined egg yolk lecithin, 0 to 50 g of the pharmaceutical glycerin, 0 to 100 g of camelina oil and 0 to 200 g of salad oil, and the purified water is added till 1000ml. The total content of fat is not less than 80 percent, wherein the MCT is not less than 20 percent. The oral preparation mainly reinforces the thermal energy as well as can regulate the blood fat and improve the energy metabolism status. The oral preparation is mainly used for health care and intestinal nourishment and used to remedy the primary malnutrition and the pathological malnutrition, which is capable of promptly improving the energy and nourishment supply status, improving the antiviral ability, strengthening the immunity function, reducing the complications, shortening the time of being in hospital, reducing the treatment cost and improving the clinically comprehensive curative effect.
CA2223573C Use of hydroxyethyl starch to prevent post surgical adhesion and as an intracavity carrier device Hydroxyethyl starch (HES) and use thereof in methods are provided for reducing or preventing adhesion formation between tissue surfaces, e.g., organ surfaces, in body cavities following surgical procedures and for drug delivery. HES may be used as an absorbable mechanical barrier alone or in combination with one or more anti-adhesion formation compounds for application to injured areas of tissues, e.g., organs, situated in body cavities such as the peritoneal, pelvic, pleural cavity, central nervous system and interligamentous space. HES may also be used as an intracavity carrier device for delivery of pharmaceutically active agents.
CN102000054A Flavone analog, preparation and application thereof as anti-diabetic medicament The invention discloses a flavone analog and application of a pharmaceutically acceptable salt thereof to preparation of an anti-diabetic medicament. The flavone analog has a structure shown by a formula I-X or II-X, wherein R1 in the formula I-X or II-X is selected from a substituted phenyl group, a substituted or unsubstituted furan group and a substituted or unsubstituted thienyl group and the substituent group is selected from a C1-4 alkyl group, a C1-4 alkoxyl group, halogen, a hydroxyl group and a cyano group; R2 is selected from the substituted phenyl group, the substituted or unsubstituted furan group and the substituted or unsubstituted thienyl group and the substituent group is selected from the halogen, the hydroxyl group and the cyano group.
CN103417569A Drug for treatment of burns and scalds and application method thereof The invention relates to a drug for the treatment of burns and scalds and an application method thereof and belongs to novel applications of drugs made from pure chemical materials. The drug is made with 10-25g of Al(OH)3, 5-15g of KNO3, 15-20g of Na2CO3, and 8-20g of NaCl; the components weighed according to a prescription are ground into 150- to 200-mesh powders, and the powders are mixed well; water is blended to the mixture according to the weight ratio of 1:20-30. The application method of the drug includes: immersing a burned or scaled part of a patient in 800-1200ml of emulsion solution until the patient feels no pain when the burned or scalded part is taken out. The drug is simple to make, low in cost and convenient to use; after healing with the drug, no scar is left; the requirements for treatment condition are low.
CN103340922A Foot soaking liquid and preparation method thereof The invention discloses a foot soaking liquid. The foot soaking liquid comprises trace elements, magnesium element, potassium element, alkaloid, emulsifying agent and water, wherein the trace elements include Fe, B, Mn, Zn, Cu and Mo. The foot soaking liquid is used for treating foot diseases such as tinea pedis, foot odor and the like.
WO2012050735A1 Methods and dosage forms for the treatment of human cancers Methods for the treatment of human cancers, daily dosage forms for cancer patients, and methods of formulating the dosage forms are provided wherein the daily dosage form contains from about 10-6,000 mg of each of β-sitosterol, iso vanillin, and linolenic acid. Preferably, the dosage forms are formulated by first creating an aqueous decoction of Arum palaestinum Boiss, followed by fortification of the decoction with additional quantities of β-sitosterol, isovanillin, and linolenic acid.
EP1089735B1 4-benzyl piperidine alkylsulfoxide heterocycles and their use as subtype-selective nmda receptor antagonists Novel 4-Benzyl piperidine alkylsulfoxide heterocycles are disclosed and their use as subtype selective NMDA receptor antagonists, particularly for the treatment of Parkinson's disease, most preferably in combination with L-DOPA.
WO2014140410A1 Composition for oral administration for binding aldehydes in the gastrointestinal tract The present invention relates to a non-toxic composition containing one or more cysteine compounds selected from L- or D-cysteine, N-acetyl cysteine, and the pharmaceutically acceptable salts thereof, for decreasing the risk of a subject contracting cancer of the stomach, the small intestine and the colon, by locally binding aldehydes present in the stomach, and optionally also separately the aldehydes carried to the small intestine or the colon, or both, whereby the composition is formulated with the help of two or more additives into controlled-release tablets containing at least one additive selected from cationic and gel- forming polymers, which tablets are formed from two or more separate layers with different release profiles, whereby the cysteine compounds are added both into the inner layer(s) and into the tablet material surrounding these.
WO2013012692A1 Pharmaceutical compositions comprising plant-based polysaccharides and uses thereof A composition for providing relief to a discomfort of an eye comprises a pharmaceutically acceptable carrier and a polysaccharide extracted from a plant source, In certain embodiments, such a polysaccharide can be extracted from mushrooms, such as from the Tremella fuciformis species. The composition is administered to an affected eye to provide such relief or discomfort.
CN102949347A Docetaxel-coated polylactic-co-glycolic acid (PLGA) nano particles and preparation method thereof The invention discloses docetaxel-coated polylactic-co-glycolic acid (PLGA) nano particles and a preparation method thereof. The nano particles comprise the following components in percentage by weight: 0.01 to 20 percent of docetaxel, 0.5 to 30 percent of PLGA and the balance of medicinal auxiliary materials, wherein the medicinal auxiliary materials comprise cyclodextrin, polyvinyl alcohol (PVA) and lecithin. The method comprises the following steps of: dissolving inclusion compound freeze-dried powder of cyclodextrin-coated docetaxel into an aqueous solution of the PVA, and dripping the PLGA into an oil phase formed by dichloromethane to form W/O initial emulsion; and dripping the initial emulsion into the aqueous solution of the PVA, emulsifying to form W/O/W complex emulsion, distilling under reduced pressure to remove the dichloromethane, stirring under an ice bath condition to obtain a nano particle solution, centrifuging, washing and redissolving the collected nano particles, performing vacuum freeze drying, and thus obtaining the docetaxel-coated PLGA nano particles. The docetaxel-coated PLGA nano particles have high encapsulation efficiency, medicament loading capacity and stability; and the dissolution degree and the utilization rate of an oral preparation of the docetaxel can be effectively improved.
WO2006137546A1 Treatment method for preventing transplantation tissue with biological origin from calcification and tissue treated thereby It is intended to provide a tissue for transplantation being free from troubles accompanying transplantation such as calcification. It is also intended to provide a membrane for preventing adhesion by which adhesion caused by a surgical operation or treatment can be prevented. It is found out that when a biocompatible polymer is added to an untreated tissue and then the tissue is exposed to Ϝ-ray irradiation, the tissue is unexpectedly strengthened and calcification is prevented, thereby solving the above problems. Although there has been recognized that decellularization is the key factor in preventing a tissue with a biological origin from calcification, it is indicated that Ϝ-ray irradiation is more efficacious than decellularization. Namely, a membrane for preventing adhesion, by which adhesion can be prevented without inducing troublesome reactions (for example, calcification, an inflammatory reaction, unnecessary cell migration or adhesion, platelet aggregation, acceleration of blood coagulation, etc.), is provided.
WO2008122352A1 Imidazolidine carboxamide derivatives as lipase and phospholipase inhibitors The invention relates to imidazolidine carboxamide derivatives of general formula (I) having the meanings indicated in the description, the pharmaceutically usable salts thereof, and the use thereof as medicaments.
CN101591276B Method for preparing bumetanide The invention relates to a method for preparing bumetanide, which comprises that: 3-amino-4-phenoxy-5-sulfonylaminobenzoic acid and n-butanal are used as raw materials; firstly, the raw materials are subjected to condensation-dehydration reaction in the presence of a boron trihalide ether catalyst to generate 3-butylimine-4-phenoxy-5-sulfonylaminobenzoic acid; and then, the 3-butylimine-4-phenoxy-5-sulfonylaminobenzoic acid is catalyzed by palladium carbon and hydrogenated to form the bumetanide. The method has the advantages of simple operation, short reaction time and low equipment requirement, and is suitable for industrialized production; and the yield of a target product can reach more than 90 percent.
US8221794 Anti-angiogenic nanoparticle compositions The present invention provides compositions comprising an anti-angiogenic factor, and a polymeric carrier. Representative examples of anti-angiogenic factors include Anti-Invasive Factor, Retinoic acids and derivatives thereof, and paclitaxel. Also provided are methods for embolizing blood vessels, and eliminating biliary, urethral, esophageal, and tracheal/bronchial obstructions.
CN1593395A Sobering agent prepared by acetyl cysteine The invention discloses a sobering agent prepared by acetyl cysteine, which is prepared by mixing acetyl cysteine with edible solvents such as beverage, foodstuff and starch tablet into various taste, various shape of single or compound dosage type. The sobering agent can help people achieve the goal of preventing drunk or reduce drunk degrees.
WO2012162463A1 Benzothiazolyl inhibitors of pro-matrix metalloproteinase activation This invention relates to benzothiazole (formula I) and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, and R6 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
US20110160148 Novel Diverse Lead Compound Autotaxin Inhibitors Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include naphthalenesulfones, phenylsulfones, and certain peptides with unnatural amino acids and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.
US20090197928 Novel Receptor Antagonists and Their Methods of Use The present invention relates to novel isoxazole derivatives of formula (I) which bind to the P2X7 receptor and are capable of interfering with the effects of ATP at the P2X7 receptor: and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
CN101862343A Application of luteolin 3'-glucoronide to preparing anti-hepatitis B virus medicine The invention relates to application of luteolin 3'-glucoronide to preparing an anti-hepatitis B virus medicine expressed in formula (1). The luteolin 3'-glucoronide has no obvious toxicity on host HepG2.2.15 cells, wherein, the maximum non-toxic concentration TC0 is more than 500 mu g/ml on the HepG2.2.15 cells; the luteolin 3'-glucoronide has obvious inhibition effect on expressing HBeAg and HBsAg by the HepG2.2.15 cells; and after being cultured for 9 days by growth solution containing 500 mu g/ml of a compound in formula (1), the contents of HBeAg and HBsAg in cell supernatant are respectively 51% and 70% of a control group (i.e. the inhibition ratios are respectively 49% and 30%) as shown in formula (1).
CN102614192A Medical composition for emergency contraception The invention relates to a dosage regimen for emergency contraception and a medical composition for the dosage regimen. In the dosage regimen for emergency contraception existing in the prior art, a single dose of 10 mg of mifepristone is taken within 120 hours of sexual intercourse, especially within 72 hours, the contraceptive effect is not good. The dosage regimen for emergency contraception with good contraceptive effect provided by the invention is characterized in that 5 mg +/- 0.5 mg of mifepristone dose unit is taken within 120 hours of sexual intercourse, and 5 mg +/- 0.5 mg of mifepristone dose unit is taken again within 12 hours of sexual intercourse. The technical scheme of the invention can effectively prevent pregnant, and especially has better contraceptive effect of taking medicine within 72-120 hours than the single dose, and the side effect is little.
WO2011079807A1 Dipropofol pyrophosphate dihydrogen ester and pharmaceutically acceptable salt, preparation process and application thereof Dipropofol pyrophosphate dihydrogen ester and pharmaceutically acceptable salt, preparation process and application thereof. The ester (2) is prepared by phosphorylating propofol with P2O5 as phosphorylating reagent in anhydrous organic solvent at 25-110°C for 2-8h under stirring, and condensing to obtain white solid. The title pharmaceutically acceptable salt is prepared by salifying ester (2) with base in organic solvent at 0-80°C for 1-5 h under stirring, filtering to obtain white solid. The process has the advantages of simple preparation process, high product yield and purity, low cost, and easily-accessible raw materials. The ester (2) and its pharmaceutically acceptable salt may be used to prepare the medical preparations as sedative, hypnotic and anesthetic, with stable property and good water solubility.
CN103006625A Application of mannitol in preparation of anti- pancreatic cancer drug The invention discloses an application of mannitol in preparation of an anti-pancreatic cancer drug, and in particular relates to a use of a mannitol injection with a specific concentration of 10%-19% for treating pancreatic cancer. Traditionally, mannitol is only used as a diuretic, a high-permeability hypotensor and the like, while the inventor discovers through scientific experiments that mannitol has anti-tumor activity, and through several cell apoptosis detection technologies and by detecting apoptosis-related genes bcl-1, and bax, proves that the specific-concentration mannitol can induce various human cancer cell strains to generate obvious cancer cell apoptosis, grasps the effect relation with concentration and time, and first illustrates the possible mechanism; furthermore, the inventor has used the research result for tumor patient treatment and has achieved obvious curative effect, which provides theoretical basis and practical cases for the application of mannitol in preparation of the anti-tumor drug and the clinical generalization thereof.
WO2012075754A1 Pharmaceutical composition for treating acute lymphocytic leukemia The present invention discloses a pharmaceutical composition for treating acute lymphocytic leukemia which comprises 6-shogaol and Salubrinal. The combination of 6-shogaol and Salubrinal in low dose can obtain the biological effect of 6-shogaol in high dose, and can significantly reduce the clinical dose of 6-shogaol, and decrease the occurrence of the potential toxicity and side effect, and can increase the safety index of clinic therapeutics.
WO2007125203A1 Gem-difluoride c-glycopeptide compounds, their preparation and use particularly for preservation of biological materials. The invention relates to a gem-difluoride C-glycopeptide compound with formula I where n is an integer equal to 3 or 4, R represents a hydrogen atom, an alkyl, benzyl, acetyl, trimethylsilyl, tert-butyldimethylsilyl, tert-butyldiphenylsilyl group, R´ represents OR, NR'R'', N3, or a phthalimide, R' and R'' represent a hydrogen atom or an alkyl, aryl, benzyl, benzoyl, acetyl, alkyloxycarbonyl, allyloxycarbonyl, benzyloxycarbonyl group, R1 represents a hydrogen atom or an alkyl, benzyl, alkylcarbamate, allylcarbamate, benzylcarbamate, acetyl group, R1 may consist of an amino acid if R2 represents only OR, R2 includes an amino acid if R1 represents a hydrogen atom or an alkyl, benzyl, alkylcarbamate, allylcarbamate, benzylcarbamate, acetyl group, R2 represents OR when R1 represents an amino acid, R3 represents a hydrogen atom or a free or protected alcohol function. It is applicable to the preparation of compounds or compositions to be used for preservation of biological materials such as cells, tissues and organs at various temperatures.
WO2008152173A1 Phenolic extracts of almond peel containing procyanidins, propelargonidins and prodelphinidins, and method for preparation thereof This invention concerns phenolic extracts containing procyanidins, propelargonidins and prodelfinidins obtained from peel of the almond [Prunus dulcís (Mili.) D.A. Webb, Prunus amygdalus (L.) Batsch., Amygdalus dulcís (Mili.), Amygdalus communis (L.) or Prunus communis (L.)]. In particular, the objective is to obtain extracts rich in proanthocyanidins with type-A bonds. The preparation method for which protection is also claimed consists in: a) a maceration of plant material with organic solvents at 25-100 °C, b) purification by liquid-liquid extraction and/or adsorption or ion exchange chromatography, and c) optionally, a final drying. Also protected are the possible activities/properties of these extracts such as anti-oxidant activity and others, which determine the use thereof as a nutritional or health ingredient, and the use thereof in the cosmetic and pharmaceutical industry.
WO2010129406A3 Methods of promoting muscle growth The present invention relates to use of the interaction of myostatin with the activin type II receptors, and more specifically to use of soluble ACVR2 to increase muscle growth in a subject. As such, methods of increasing muscle mass in a subject are provided. In addition, methods of ameliorating the severity of a pathologic condition characterized, at least in part, by a decreased amount, development or metabolic activity of muscle are provided.
CN101683330A Oral compound pharmaceutic preparation containing tranilast and salbutamol The invention relates to an oral compound pharmaceutic preparation for treating asthma, which contains tranilast shown as the formula (I) and salbutamol sulfate shown as the formula (II) or other pharmaceutically allowed active ingredients. The invention also relates to the application of compounds shown as formulas (I) and (II) or pharmaceutically allowed salts thereof in the preparation of an oral therapeutical agent for treating asthma.
CN103126997A Sustained release microsphere containing risperidone and risperidone analogues and preparation method thereof The invention provides a sustained release microsphere containing risperidone and risperidone analogues and a preparation method thereof, wherein the sustained release microsphere containing the risperidone and the risperidone analogues can be used for injections. The sustained release microsphere comprises an active substance risperidone, the risperidone analogues, biodegradable medicinal high polymer materials, plasticizers, antioxygen and the like. The preparation method of the sustained release microsphere containing the risperidone and the risperidone analogues can be an emulsion process, a spray drying process, a low-temperature spray extraction method, a supercritical fluid method and the like. A blank medicinal high polymer material layer can also be wrapped on the surface of the microsphere on the basis. The microsphere preparation solves the problems, of dumping, lag phase and the like, existing in a reported or a listed product. The composition is mainly used in treating acute and chronic mental diseases.
CN102100687B Application of medicine composition with function of exterminating oral helicobacter pylori The invention relates to an application of polylysine in a preparation of medicine composition with a function of exterminating oral helicobacter pylori. The polylysine and a glycerol monolaurate are simultaneously used, the cure rate of exterminating the oral helicobacter pylori of 83%, also reduces the infection and relapse rate of the gastric helicobacter pylori, does not hurt oral tissues and does not have toxic or side effects.
EP1303304B1 Pharmaceutical combinations for treatment and prevention of diabetes mellitus Pharmaceutical combinations for treatment and/or prevention of all sorts, periods and complications of diabetes mellitus in mammals, thus including the pre-diabetic diseases and their complications, optionally including furthermore ischaemic heart disease comprising an effective dose of at least one enzymatic nitric oxide (NO) donor active ingredient and optionally comprising an effective dose of at least one antidiabetic active ingredient, and further optionally comprising usual pharmaceutically acceptable carriers and/or other auxiliaries. The combination may consist of more than one pharmaceutical compositions. The effective doses related to the new insulin-sensitizing effect are considerably lower than the usual doses related to the known effect of most active substances dues to metabolic effects that influence insulin sensitivity in healthy and insulin resistant mammals. The usual dose of NO-donors is necessary when the patient has also ischaemic heart disease. Preferred antidiabetics include insulin, a thiazolidinedion, a biguanide derivative, an α-glucosidase-inhibitor, an α2-adrenergic-antagonist and/or a sulphonamide, preferably a sulphonylurea. Preferred enzymatic NO donors are nitroglycerin, racemic isosorbide monoitrate, and/or its stereroizomers, racemic isosorbide dinitrate and/or its stereoizomers, erythrityl tetranitrate, pentaerythritol-tetranitrate, methylpropyl-propanediol-dinitrate, propatyl nitrate, trolnitrate, tenitramine and/or nicorandile. The invention includes methods of treatment and processes to prepare the compositions.
WO2007097697A1 Therapeutic quinoline compounds that are 5ht1b modulators The present invention provides compounds having formula (I): wherein the compounds are useful for the treatment of anxiety disorders, cognitive disorders, and/or mood disorders. The compounds are 5HT1B modulators.
CN101028400A Xue Shang Hua embrocation and its production An exterior-applied 'Xueshanghua liniment' in the form of tincture, oil, liquid, dressing, or ointment is prepared from 18 Chinese-medicinal materials including notoginseng, safflower, rehmannia root, borneol, etc.
CN102847152A Inhalation preparation containing N-acetyl-L-cysteine and glucocorticoid, and its preparation method The invention discloses an inhalation preparation containing N-acetyl-L-cysteine and glucocorticoid, and its preparation method. Active ingredients (N-acetyl-L-cysteine and glucocorticoid) and one or more pharmaceutical adjuvants suitable for inhalation constitute the inventive preparation.
US8486698 Inducing differentiation of an isolated marrow stromal cell into a neuronal cell tissue engineering for use in prevention and treatment of nervous system disorders; regenerative medicine; tissue engineering The present invention relates to methods of inducing differentiation of mammalian bone marrow stromal cells into neuronal cells by contacting marrow stromal cells with a neuronal differentiation-inducing compounds. Neuronal differentiation-inducing compounds of the invention include anti-oxidants such as, but not limited to, beta-mercaptoethanol, dimethylsulfoxide, butylated hydroxyanisole, butylated hydroxytoluene, ascorbic acid, dimethylfumarate, and n-acetylcysteine. Once induced to differentiate into neuronal cells, the cells can be used for cell therapy, gene therapy, or both, for treatment of diseases, disorders, or conditions of the central nervous system.
EP1511759A1 Modulators and inhibitors of fibroblast growth factor receptor 5-polypeptides and gene expression thereof. Isolated fibroblast growth factor receptor (FGFR5) polypeptides and polynucleotides encoding such polypeptides are provided. Also provided are modulators of FGFR5 gene expression and binding molecules that specifically bind to and agonize or antagonize FGFR5 polypeptide function. Specific binding molecules include antibodies, functional fragments thereof, as well as scFv and Camelidae heavy chain IgG that specifically bind to FGFR5 thereby modulating the activity of FGFR5 and, thus, are effective agents suitable for the treatment of diseases such as osteopontin-mediated autoimmune disease, such as systemic lupus erythematosus, bone disorders including osteoporosis and osteopetrosis, and cancers, including cellular carcinomas such as hepatocellular carcinomas.
US20120021989 Genetic markers for risk management of atrial fibrillation and stroke The invention relates to procedures and methods of determining a susceptibility to cardiac arrhythmia, including Atrial Fibrillation, Atrial Flutter and Stroke, by assessing the presence or absence of alleles at polymorphic markers found to be associated with risk of these conditions. The invention further relates to kits encompassing reagents for assessing such markers, and diagnostic 5 methods, uses and procedures for utilizing such susceptibility markers.
CN103356577A Application of Sarcaboside A in preparation of drug for treating stomach cancer The invention discloses application of Sarcaboside A in preparation of a drug for treating stomach cancer, which belongs to the technical field of new applications of drug. According to the invention, the in-vitro MTT (Methyl Thiazolyl Tetrazolium) antitumor activity evaluation discovers that Sarcaboside A also has an obvious inhibiting effect on the growth of human stomach cancer cell strains HGC-27, MGC-803, BGC-823 and SGC-7901. Thus, Sarcaboside A can be used for preparing an anti-stomach cancer drug and has good development and application prospects. The application of Sarcaboside A in preparation of the drug for treating stomach cancer is disclosed by the invention for the first time. The skeleton type is brand new and Sarcaboside A has unexpectedly high inhibitory activity on the human stomach cancer cell.
CN102617599A Macrocyclic compound and application thereof The invention relates to the field of biological medicine, particularly to a macrocyclic compound, namely a compound with a general formula (I), and pharmaceutically acceptable equivalent or salt. The invention further relates to a preparation method of the compound with the general formula (I) and the use of such novel pyrimidine compound, particularly to the use of the compound as Janus kinase restrainer. The macrocyclic compound is used in but not limited to real red erythrocytosis, spontaneous thrombocytosis, chronic and idiopathic myelofibrosis, myelogenic metaplasia with myelofibrosis, chronic myelocytic leukemia, chronic bone marrow mononuclear cell leukemia, tranformation reaction, asthma, and autoimmunization diseases such as transplant rejection restrain, chronic infectious arthritis, muscle shrinkage lateral sclerosis, multiple sclerosis and material solid and blood malignancy such as lymphocytic leukemia, and lymphoma.
WO2008029282A3 Aqueous formulation comprising an antitumor agent Disclosed are compositions and pharmaceutical formulations comprising (2R)-2- [4-(7-bromo-2-quinolyloxy)phenoxy]propanoic acid, and methods of use thereof.
CN101129908B Antitussive of Miao national herbs bile prime and method of preparing bile prime The invention discloses a bilineurin cough-relieving miao medicament, which is prepared from pig's bile or ox bile through inducing Qian penicillin 2000-1 bacterial for fermentation, extracting powdery bile essence, than mixing with ardisia japonica, cordate houttuynia, arctium fruit, root of ballon flower, roor of sessile stemona, isatic root, Sichuan fritillary bulb and auxiliary materials. The invention also discloses the process for preparing the medicament, which has the functions of anti-inflammation for treating cough, sterilizing, resisting viruses, reducing phlegm and relieving cough quickly and effectively. It adopts pig's bile or ox bile as the main content of relieving cough, rather than the snake bile as traditionally used for thousands of years. Therefore, it can prevent from killing in large scale all kinds of snakes protected by country, it is good to protect and balance the ecological environment, and has huge social and economic benefit.
EP1423166B1 Non-peptide ccr1 receptor antagonists for the treatment of progressive renal fibrosis This invention is directed to pharmaceutical compositions useful in treating progressive renal fibrosis in mammals comprising a pharmaceutically acceptable excipient and a therapeutically effective amount of a non-peptide CCR1 receptor antagonist.
CN103450281A 1-azabenzanthrone-platinum (II) complex as well as synthesis method and application thereof The invention discloses a new 1-azabenzanthrone-platinum (II) complex, i.e., monochloro.mono(dimethyl sulfoxide).mono(1-azabenzanthrone) platinum (II), as well as a synthesis method and an application thereof. The complex is prepared through the following steps: weighing equivalent amounts of 1-azabenzanthrone and dichloro-di(dimethyl sulfoxide) platinum (II); dissolving in a polar solvent; heating or performing reflux reaction to obtain a target product, wherein the synthesis can specifically be performed through a solution method or a solvothermal method. Investigation shows that the complex has anti-proliferative activity on human tumor cell strains such as HepG2, SK-OV-3, SK-OV-3/DDP, BEL-7404, T-24 and HL-7702; the result shows that the complex has obvious in-vitro anti-tumor activity, has higher potential medicinal value and is expected to be used for preparing various anti-tumor medicaments. The chemical structural formula of the complex is shown in the specification.
WO2008059029A3 New polymorphs of ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1h-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate The invention relates to new polymorphs of the active substance ethyl 3-[(2-{[4- (hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H- benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate, the preparation thereof and the use thereof as pharmaceutical compositions.
WO2013104263A1 Synthesis of polyhydroxy benzopyran ketone compound and anti-tumor effect thereof Provided is a polyhydroxy benzopyran ketone compound having the structure as represented by formula (I) and pharmaceutically acceptable salt or pro-drug thereof, as well as pharmaceutical composition containing the compound. The compound can be used to regulate and control a novel estrogen receptor ER-α36，and to prevent and/or treat the diseases related to ER-α36 receptor-mediated tumors, such as breast cancer, leukemia and liver cancer and the like.
US20050281864 comprises fatty acids; for treatment/prevention of sepsis or inflammatory shock A composition for use as a medicament, functional food or nutritional product is described which comprises at least one lipid wherein the lipid provides greater than 35% total energy of the composition. A preferred embodiment comprises a n-6/n-3 fatty acid ratio of about 2/1 to 7/1. In addition, a method of preparing the composition; use of the composition in the manufacture of a medicament, functional food or nutritional product; and a method of treatment or treatment or prevention of sepsis or inflammatory shock which comprises administering an effective amount of the composition are described.
CN103371980A Dexamethasone sodium phosphate freeze-dried powder injection The invention relates to a dexamethasone sodium phosphate freeze-dried powder injection. Every bottle contains 1-20mg of dexamethasone sodium phosphate, 20-150mg of excipient and pH regulator. The components in the formula are dissolved in a solvent and freeze-dried to obtain the powder injection. The invention is characterized in that the solvent is ethanol-containing water for injection, and the liquor prepared by dissolving the components in the formula in the solvent contains 5-10 vol% of ethanol.
WO2011067166A1 Azacyclic spiro derivatives Compounds of Formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein R1, R2, R3 and n have the significance given in claim 1.
CN1980656B New pharmaceutical use of lipase inhibitor The present invention provides lipase inhibitors containing dimers having an epigallocatechin gallate (EGCG) unit derived from teas as well as foods and beverages and medicines containing the inhibitors. More specifically, the present invention provides lipase inhibitors containing at least one of proanthocyanidins represented by the formula 1: wherein R1 and R2 independently represent H or OH, and R3 and R4 independently represent H or a galloyl group; as well as foods and beverages and pharmaceutical compositions containing said lipase inhibitors.
US20070293579 Use of carp inhibitors for the treatment of heart diseases The present invention relates to the novel finding that inhibition of human CARP protein or of CARP DNA/mRNA may successfully cure heart disorders, especially heart failure in humans. The invention relates, therefore, to pharmaceutical compositions containing substances, preferably of lower molecular weight, which may influence the activity of cardiac CARP. The invention relates, furthermore, to a method of treatment heart failure using CARP inhibitory compounds, to methods for screening these inhibitors and to the use of CARP as diagnostic tool.
WO2010065760A1 Imidazo [1,2a] pyridine derivatives, their use as s1p1 agonists and methods for their production The invention is directed to Compounds of Formula (I) as well as methods of making and using the compounds.
CA2862030A1 Apoptosis signal-regulating kinase inhibitor The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase ("ASK 1") inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.
US20090012494 Intradermal delivery of biological agents The present invention relates to methods for intradermally delivering one or more biologically active agents such as vaccines and therapeutic agents into the dermis layer of the skin of a subject to obtain systemic delivery or an immune response using a microneedle drug delivery device containing the agent to be delivered. The methods employ a microneedle device with a row of hollow microneedles. The microneedles penetrate the skin of the subject and assume an anchored state in which the microneedles are anchored in the skin and project laterally from the device. A pivotal motion is then performed with the device so that the skin in which the microneedles are engaged is lifted above the initial plane of the surface of the skin while the biologically active agent is delivered. The methods of the invention elicit increased humoral and/or cellular response as compared to conventional vaccine delivery routes, facilitating dose sparing.
CN103550355A Anus relaxing health ointment and preparation method thereof The invention provides an anus relaxing health ointment and a preparation method thereof. The anus relaxing health ointment mainly comprises the following raw materials in parts by weight: 15 parts of snake gall, 15 parts of phellodendron amurense, 15 parts of coptis chinensis, 16 parts of brown sugar, 17 parts of scorpion, 10 parts of centipede, 20 parts of mirabilite, 20 parts of alumen, 15 parts of mature vinegar, and 180 parts of sesame oil. According to the preparation method, snake gall, phellodendron amurense, mature vinegar, coptis chinensis, brown sugar, scorpion, sesame oil, centipede, mirabilite and alumen are selected and combined; the medicines work synergistically and realize the functions of strengthening a drug and treating dyschizia, bearing-down pain of rectum and enabling the mass to be taken off, so that the haemorrhoids can be treated effectively.
CN102114014A Pharmaceutical composition containing almotriptan The invention discloses a pharmaceutical composition containing the active ingredients of almotriptan or its salts. The pharmaceutical composition can be prepared into tablets by the method of co-crushing, and can be used for treating migraine symptom.
WO2011034912A1 Compositions and methods for treating spasticity Disclosed are methods of treating spasticity by administering to a patient in need of such treatment a compound having formula (I).
US20110281850 Intracellular kinase inhibitors Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.
CN101434558A Salicylic acid-sphingoid base derivative and uses thereof The invention relates to a compound which is a derivative of salicylic acid-analog sphingosine base, wherein, the salicylic acid is coupled to the analog sphingosine base in Formula (1) by amido links, while A is CH2-CH2, CH=CH or C (H) OH-CH2 and R is a linear chain with 10 to 22 carbon atoms or branched alkyl and optionally contains one or more double bonds and/or is optionally replaced with one or more hydroxyl groups. And optionally, one or more glycosyl parts, or acid ester or sulfuric acid ester groups can be connected to a primary hydroxyl. The invention also relates to a preparation method of the compound, cosmetic composition and dermatology composition containing the compound, and applications of the compound as medicines and cosmetics.
US20110269764 Therapeutic approaches for treating alzheimer disease and related disorders through a modulation of synapse function The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate synapse function for treating said disease.
CA2242562C Human dnase resistant to actin inhibition This invention relates to a novel human deoxyribonuclease, referred to as LS-DNase, that is relatively resistant to inhibition by actin, as compared to human DNase I. The invention provides nucleic acid sequences encoding LS-DNase, thereby enabling the production of LS-DNase by recombinant DNA methods in quantities sufficient for clinical use. The invention also relates to pharmaceutical compositions and therapeutic uses of LS-DNase.
CN103408546A 2-phenylaminopurine PLK1 (Polo-like kinase 1) inhibitors and applications thereof The invention relates to the field of medicinal chemistry, and in particular relates to 2-phenylaminopurine compounds, a preparation method for the compounds, a medicinal composition containing the compounds, and medical applications for the compounds, and in particular an application for the compounds as Polo-like kinase 1 inhibitors.
WO2009120803A3 Water soluble small molecule inhibitors of the cystic fibrosis transmembrane conductance regulator Provided herein are highly water soluble, thiazolidinone derivative compounds and glycine hydrazide derivative compounds that inhibit the ion transport activity of the cystic fibrosis transmembrane conductance regulator (CFTR). The compounds, and compositions comprising the compounds, described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea. The compounds may also be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.
EP1200321B1 Valve with a valve stem wiper There is provided a valve for an aerosol container. The valve comprises a valve body (1); a valve stem (7) having a dispensing passage (15), and contacting said valve stem (7), a sealing ring (9, 12) including a sealing portion; the valve stem (7) being slidably movable relative to the sealing ring (9, 12) from a valve-closed position to a valve-open position in which the interior of the valve body is in communication with the dispensing passage (15). The sealing ring (9, 12) further includes a wiper (130) to wipe the valve stem. Preferably, the valve is a metering valve.
US20110160281 RNA Interference Mediated Inhibition of Vascular Cell Adhesion Molecule (VCAM) Gene Expression Using Short Interfering Nucleic Acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating vascular cell adhesion molecule gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of vascular cell adhesion molecule gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of vascular cell adhesion molecule genes, such as vascular cell adhesion molecule-1 (VCAM-1).
CN103127045A Composition containing gamma-aminobutyric acid and lycopene and preparation method thereof The invention provides a composition containing gamma-aminobutyric acid and lycopene. The composition contains the lycopene, the gamma-aminobutyric acid, beewax, safflower oil and walnut oil. The invention further provides a preparation method of the composition, soft capsules containing the composition and a preparation method and application of the soft capsules. The composition has good stability, and under the normal-temperature condition, storage period can be 2 years. The soft capsules have good stability, and under the normal-temperature condition, storage period can be 2 years.
US7449581 6-Substituted pyrido-pyrimidines The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.
US20080058353 Using 3-(7-(2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-1,2,3triazolo(4,5)pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane( 1 ,2-diol The present invention relates to pharmaceutical compositions and, more particularly, to a pharmaceutical composition containing the compound {1S-[1α, 2α, 3β (1S*,2R*),5β]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol.
US20080312298 Methods for Identification of Modulators of Carm1 Methyl Transferase Activity This invention relates to CARM1, CARM1 binding pockets, or CARM1-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to CARM1 protein, complexes of CARM1 protein, homologs thereof, or CARM1-like protein or protein complexes. The invention also relates to crystallizable compositions and crystals comprising a CARM1 protein or homologs thereof. The invention also relates to methods of identifying binders of CARM1 proteins. The invention also relates to methods for determining the intracellular activity of CARM1 methyltransferase and methods for identifying an agent that inhibits the intracellular activity of CARM1 methyltransferase.
WO2014140284A1 Use of linagliptin in cardio- and renoprotective antidiabetic therapy The present invention relates to the DPP-4 inhibitor linagliptin for use in cardio- and/or renoprotective therapy, including in diabetic or non- diabetic patients at high vascular risk.
WO2008089776A1 Formulation of and method for producing an infusion rehydration solution The invention relates to the formulation of, and a method for producing an infusion rehydration solution for the treatment of (i) energy deficiencies corrected with the addition of glucose to the blood and (ii) hydric imbalances with the provision of water and mineral salts.
WO2008010238A2 Antidiabetic azabicyclo [3. 1. 0] hexan compounds The present invention provides novel compounds of the general formula (I), wherein the symbols are same as described in specification, their pharmaceutically acceptable salts, their tautomeric forms, their stereoisomers, pharmaceutical compositions containing them, to process and intermediates for the preparation of the above said compounds, having the utility of these compounds in medicine and to methods for their therapeutic use, and their use in the treatment of diabetes and related diseases.
CN101869569A Ready-to-use entecavir composite The invention discloses a low-dose ready-to-use entecavir composite, belonging to the pharmaceutical field. The low-dose ready-to-use entecavir composite is a liquid pharmaceutical composition containing entecavir; the pH value of the composite is 3-7; and the composite comprises the following components: a) 0.001%-20% (w/v) of entecavir in proper pharmaceutically acceptable solvent; b) 0.01%-10% (w/v) of sweetener; and c) 0.01%-5% (w/v) of buffering agent. The low-dose ready-to-use entecavir composite has the advantages of high palatability, good stability and easy quantitative method and taking way.
CN103382195A Benzopyran chalcone compound, and preparation method and application thereof The invention relates to the fields of organic chemistry and pharmaceutical chemistry, specifically to a benzopyran chalcone compound having anti-inflammatory activity and a preparation method and application thereof. The benzopyran chalcone compound has a structure as described in the specification. According to results of experiments, the compound has inhibiting effects on inflammatory factors like iNOS, TNF-alpha and IL-4 and can be used for treating inflammations like osteoarthritis, rheumatoid arthritis and asthma.
WO2007039809A1 Metabolites of 2- {3-[4-(5-fluoro-2-isopropoxy-phenyl)-piperazin-1-yl]-propyl} -5,6-dihydroxy-hexahydro-isoindole-1,3-dione The present invention relates to metabolites of 2-{3-[4-(5-fiuoro-2-isopropoxy- phenyl)-piperazin-1-yl]-propyl}-5,6-dihydroxyhexahydro-lH-isoindole-1 ,3(2H;-dione of Formula (I). The compounds described herein can function as α1a-adrenoceptor antagonists and thus can be used to treat benign prostatic hyperplasia (BPH) and related symptoms thereof. Processes for preparing such metabolites, pharmaceutical compositions thereof, and methods of treating BPH and related symptoms thereof are also provided.
CN101791314B Application of crocin in preparing hypnotic drug The invention belongs to the field of compound drugs, which relates to new drug application of crocin and a derivant thereof, in particular to application of crocin and a derivant in preparing a hypnotic drug and a health product. The crocin is ester formed by combining crocetin2-naphtholum8-sulfoacid with two-molecule gentiobiose with a chemical formula of C44H62O24 and molecular weight of 974.97. An animal experiment proves that the non-rapid eye movement sleep (slow wave sleep) time can be increased to treat insomnia or improve sleep quality, and the sleeping quantity is improved with dosedependent. The crocin and the derivant thereof can be used for preparing sedative-hypnotic drugs and health products and can be prepared into intestinal or non-intestinal combination drugs which comprise granules, tablets, liquid preparations, sustained release agents, medicinal granules, gelatin pearls, capsules or injections.
CN102002052A Ginkgolides K and compound thereof as well as preparation method and use thereof The invention discloses a compound of ginkgolides K of which a general formula is shown in (I), and a composition is prepared by mixing the ginkgolides K compound and pharmaceutically-acceptable medicine carrier, wherein G is alkaline substances. The invention also discloses a preparation method of the compound and treatment use thereof. In the invention, the ginkgolides K compound changes the physical property of the ginkgolides K, thereby the invention has the advantages of good stability, and the ginkgolides K compound has good water-solubility and higher stability. In the compound, a natural structure of the ginkgolides K can be kept, and when the compound is used as an effective component to enter the human body, the activity of the ginkgolides K can be fully developed to achieve theaim of treating an illness.
US20080221202 treatment of disorders and conditions modulated by at least one progesterone or glucocorticoid receptor; 11-(4-Dimethylamino-phenyl)-1-hydroxy-12a-methyl-1-prop-1-ynyl-1,3,4,4a,4b,5,6,9,10,11,12,12a-dodecahydro-2-oxa-chrysen-8-one The present invention is directed to novel steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by at least one progesterone or glucocorticoid receptor.
US7166722 The monohydrochloric acid salt monohydrate, and its preparation by adding hydrochloric acid to a solution of N-{2-chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl}-N'-(5-methyl-3-isoxazolyl)urea in an N,N-dimethylformamide or N,N-dimethylacetamide aprotic solvent, adding ethanol and ethanol and water The present invention provides a crystal of a pharmaceutically acceptable salt of N-{2-chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl}-N′-(5-methyl-3-isoxazolyl) urea. This crystal of salt is usable for the therapy of a disease selected from the group consisting of tumors, diabetic retinopathy, chronic rheumatism, psoriasis, atherosclerosis, Kaposi's sarcoma, and exudation type age-related maculopathy, and has characteristics suitable for applications of oral pharmaceutical preparations.
CN101798333A Tetraterpene compound and derivatives thereof for treating cancer, inflammation and central nervous system diseases The invention discloses a pentacyclic triterpene compound and derivatives thereof. The pentacyclic triterpene compound and the derivatives thereof can inhibit the growth of tumour cells and can be used to treat cancer, inflammation and central nervous system diseases. The invention also discloses a method for extracting and chemically synthesizing the pentacyclic triterpene compound and the derivatives thereof.
WO2014094645A1 Rna interference preparation for curing hbv An RNA interference preparation for curing hepatitis B virus (HBV) is interfering nucleic acid (iNA), and comprises one or more positive strands and one or more antisense strands, one or more polynucleotide chains being complementary to one or more regions of the HBV RNA. The preparation can be used to cure HBV. The iNA is of a double strand structure, and the double strand is straight, circular, circular-like, hairpin-shaped, stem-loop, unidirectional, or bi-directional. The preparation can be used to cure HBV.
WO2013132489A1 Nucleoside 5'-phosphorothioate analogues and uses thereof The invention provides particular mono- and dinucleoside 5'-phosphorothioate analogues, more particularly mono- or di- adenosine or uridine 5'-di- or tri- phosphorothioate analogues in which at least one of the bridging oxygen atoms of the phosphorothioate is replaced by a group such as -CH2-, and at least one of the non- bridging atoms or negatively-charged atoms of the phosphorothioate is either a sulfur atom or a sulfur ion; and pharmaceutical compositions thereof. These compounds are useful for treatment of neurodegenerative diseases or disorders such as Alzheimer's disease.
CN1723915A Nanometer dental caries prevention and antibiotic material, and its prepn. method and toothpaste containing the material An anti-bacterial nano-material for preventing decayed tooth is a metallic compound of nano-class hydroxyapatite, which has a molecular formula CaxMy(PO4)6(OH)2, where M is chosen from Zn, La, Ce, and Y and x+y=10. It is prepared by sol-gel method and can be used for preparing tooth-paste.
US20130017234 Implant modified with non-hydroxylated vitamin d precursors An implant to be used as medical or dental implant, comprising a metallic or polymeric base which is covered by the vitamin D precursor cholecalciferol. The implant can be obtained by direct covering of the polymeric or metallic base with a solution comprising cholecalciferol or also covering the base with the 7-dehydrocholesterol (7-DHC), and subsequently irradiated with UV light to induce the formation of cholecalciferol. Optionally, the coating of the implant may include an antioxidant such as vitamin E. This implant enhances osseointegration in compromised patients by means of the endogenous synthesis and activity of vitamin D in hard and mineralized tissue regeneration. Furthermore, a method to obtain these implants which comprises coating the surface of the implant directly with cholecalciferol or with a specific concentration of 7-DHC and irradiated with UV light to induce the formation of cholecalciferol.
EP1562575A1 Fused cycloalkyl amides and acids and their therapeutic applications for the treatment of i.a. epilepsy The present invention relates to the use of compounds of formula (I) for the treatment of epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, or movement disorders, and to provide neuroprotection.
CN103169666A Preparation method and application of halide phenolic compound solid dispersion The invention discloses a preparation method and an application of a halide phenolic compound solid dispersion, belonging to the technical field of pharmaceutical preparations. The preparation method comprises the following steps of: respectively weighing 2,5'-dibromo-4,5,2'-trihydroxybenzophenone and a carrier material in a mass ratio of (1:1)-(1:12), dissolving with an organic solvent and ensuring that the 2,5'-dibromo-4,5,2'-trihydroxybenzophenone and the carrier material are completely dissolved and uniformly mixed; heating in a water bath at 60-70DEG C, evaporating to remove the organic solvent until the mixture is viscous; freezing the mixture in a -20DEG C refrigerator; taking out, drying in a vacuum drying box for 24 hours, and when the mixture is embrittled, crushing, and filtering through an 80-mesh sieve to obtain light yellow powder namely the solid dispersion. The preparation method is simple and convenient, and the prepared solid dispersion is good in water solubility and high in dissolving speed, and can be used clinically better.
US7098241 Thiophene hydroxamic acid derivatives The (R) and (S) enantiomers of a compound of formula I are novel antiproliferative therapeutic agents. These compounds have HDAC inhibitor activity and are useful in the treatment of cancer. Also disclosed are methods of making and using compounds of formula (I), as well as pharmaceutical compositions containing compounds of formula (I).
CN103405771A Pharmaceutical composition and applications thereof The invention provides a pharmaceutical composition and applications thereof. The pharmaceutical composition comprises a calcium channel blocker or pharmaceutical acceptable salts thereof, a phosphodiesterase 5 inhibitor or pharmaceutical acceptable salts thereof, and a pharmaceutical acceptable excipient. The pharmaceutical composition provided in embodiments in the invention has significant functions on preventing or treating acute high altitude diseases, and the pharmaceutical composition has superior composition function effects on treating the acute high altitude diseases to the single phosphodiesterase 5 inhibitor. The composition of the phosphodiesterase 5 inhibitor and the calcium channel blocker has obvious synergistic effects.
US7064204 Nitrogen compounds such as 4-(5-amino-7-phenethyl-7H-pyrazolo (4,3-e)(1,2,4)triazolo(1,5-c)pyrimidin-2-yl)-phenol, used as adenosine receptor antagonists, for prophylaxis of nervous, cardiovascular, respiratory, urogenital and immune disorders New compounds having a tricyclic pyrazolotriazolopyrimidine ring structure are provided and methods of using those compounds for a variety of therapeutic indications.
CN101780075A Combined drug for treating insomnia The invention provides a use of tizanidine hydrochloride and tandospirone citrate in the preparation of a combined drug for treating insomnia. The weight ratio of a tizanidine hydrochloride derivative to the tandospirone citrate is 1-4 to 5-20. The combined drug has the advantages that: (1) from different mechanisms of action, the combined drug has the function of synergistic effect against insomnia; (2) the clinical dosage of one or two drugs can be reduced to attenuate virulence; and (3) the invention can facilitate patients to carry and take.
WO2008045566B1 Methods for dosing an orally active 1,2,4-oxadiazole for nonsense mutation suppression therapy The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.
US20100144858 Treatment of movement disorders with a metabotropic glutamate 4 receptor positive allosteric modulator An mGluR4 receptor positive allosteric modulator is useful, alone or in combination with a neuroleptic agent, for treating or preventing movement disorders such as Parkinson's disease, dyskinesia, tardive dyskinesia, drug-induced parkinsonism, postencephalitic parkinsonism, progressive supranuclear palsy, multiple system atrophy, corticobasal degeneration, parkinsonian-ALS dementia complex, basal ganglia calcification, akinesia, akinetic-rigid syndrome, bradykinesia, dystonia, medication-induced parkinsonian, Gilles de la Tourette syndrome, Huntington's disease, tremor, chorea, myoclonus, tick disorder, and dystonia.
CN1657047A Formula of calebassine dripping pills and its preparation method A dripping pill of cucurbitacin for treating metastatic hepatitis, chronic hepatitis and primary liver cancer is prepared from cucurbitacin, polyethanediol 6000, polyethanediol 400, and alcohol as cooler.
WO2012074180A1 Novel tetraazacyclododecan-tetraone derivative or pharmaceutically acceptable salts thereof, and pharmaceutical composition containing same for preventing or treating cancer The present invention relates to a novel tetraazacyclododecan-tetraone derivative or pharmaceutically acceptable salts thereof, and to a pharmaceutical composition containing same for preventing or treating cancer. The novel tetraazacyclododecan-tetraone derivative according to the present invention suppresses the growth of tumor cells through RUNX3 expression and activation, has the effect of inducing cell death as well as of inhibiting cell movement and cell invasion, and has the effect of reducing the size of tumors, and is thus capable of being effectively used as an anticancer agent.
US20070274913 Preventives/Remedies for Stress Urinary Incontinence and Method of Screening the Same An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.
US7300917 Remedy for chronic disease A remedy and/or a preventive for a chronic disease which contains an EDG-2 antagonist. Because of binding to a subtype EDG-2 of LPA receptor, an EDG-2 antagonist is useful in treating and/or preventing chronic diseases (for example, diseases caused by the progress of chronic asthma, glomerular nephritis, obesity, arteriosclerosis, rheumatoid and atopic diseases) induced and made chronic by tissue cells whose proliferation is accelerated by LPA mediated by EDG-2.
US20110098640 Visual indication of rupture of drug reservoir The present disclosure relates to methods for visualizing the opening of a drug reservoir of an implantable medical device. In particular, the present disclosure provides methods for observing the release or exposure of contents from a drug reservoir of a medical device placed within the vitreous of an eye of a subject. The methods include implanting a drug delivery device within an anatomy of a subject. The drug device includes a plurality of reservoirs, each loaded with a therapeutic agent and a marker. Furthermore, the drug delivery device comprises a plurality of barrier layers for separating the contents of one of the plurality of reservoirs from the anatomy. The method further includes irradiating at least one of the plurality of barrier layers such that at least one of the plurality of reservoirs is breached, thereby triggering release of the therapeutic agent and the marker from the device. By visually detecting release of the marker into the anatomy, release of the therapeutic agent into the anatomy is verified.
WO2012033218A1 HYDROUS CRYSTALS OF 2-O-α-D-GLUCOSYL-L-ASCORBIC ACID, POWDER CONTAINING HYDROUS CRYSTALS OF 2-O-α-D-GLUCOSYL-L-ASCORBIC ACID, METHOD FOR PRODUCING THE HYDROUS CRYSTALS, METHOD FOR PRODUCING THE POWDER, USE OF THE HYDROUS CRYSTALS, AND USE OF THE POWDER The objective of the present invention is to provide novel 2-O-α-D-glucosyl-L-ascorbic acid crystals, a method for producing the novel 2-O-α-D-glucosyl-L-ascorbic acid crystals, and use of the novel 2-O-α-D-glucosyl-L-ascorbic acid crystals. The objective is achieved by providing hydrous crystals of 2-O-α-D-glucosyl-L-ascorbic acid, a powder containing hydrous crystals of 2-O-α-D-glucosyl-L-ascorbic acid, a method for producing the hydrous crystals of 2-O-α-D-glucosyl-L-ascorbic acid, a method for producing the powder containing hydrous crystals of 2-O-α-D-glucosyl-L-ascorbic acid, a use of the hydrous crystals of 2-O-α-D-glucosyl-L-ascorbic acid, and a use of the powder containing hydrous crystals of 2-O-α-D-glucosyl-L-ascorbic acid.
CN101361705A Anti-cancer sustained release injection containing hexa-decyl choline phosphate An anticancer slow release injection containing hexa-decatyl phosphorylcholine consists of the anticancer effective quantity including hexa-decatyl phosphorylcholine and amphiphilic block copolymer hydrogel, wherein, the hexa-decatyl phosphorylcholine is partially or totally wrapped in slow release microspheres and singly exists in the slow release injection in the form of slow release microspheres or microspheres and micropowder; the amphiphilic block copolymer is selected from PLGA-carmowax-PLGA, slow release gel has temperature-sensitive gelation property, can be liquid with flowability in the environment below body temperature and can, in an idiothermous body, automatically turn into non-flowing water-insoluble gel that can be absorbed through biodegradation, thus slowly releasing medicines in local part of tumor, the slow release microspheres are beneficial to the steady and slow release of medicines, and the double slow release is favorable to controlling the tumor cell that enters dormancy stage, while the medicine that exists in the slow release gel in the form of micropowder favors relatively fast release and the control over the cell with fast appreciation. The injection can be used together with radiotherapy particles and chemotherapeutics or others.
WO2014018862A1 Pharmaceutical compositions comprising a heat shock protein inhibitor and a|purine de novo synthesis inhibitor for treating rheumatoid arthritis or cancer A pharmaceutical composition including an effective amount of the combination of: an heat shock protein (HSP) inhibitor, and a purine de novo biosynthesis inhibitor, or a pharmaceutically acceptable salt thereof. Also disclosed is a method of treating rheumatoid arthritis or cancer including administering an effective amount of the above mentioned pharmaceutical composition to a patient in need of such treatment, as defined herein.
WO2013033797A1 Pharmaceutical composition for treatment of burns and injuries of the skin and its preparation process The present invention relates to a pharmaceutical composition for the treatment of burns, bedsores, varicose ulcers and other skin lesions, consisting essentially the novelty of the combination of sodium salicylate and zinc salts, among these, preferably, zinc sulfate, at specific concentrations, and be even associated to silver sulfafdiazine, being the base of the cream constituted by cetostearyl alcohol, cetostearyl ethoxylated alcohol 20 e o; lanoline, propylenoglycol, paraffine, solid vaseline, of mineral oil, methylparaben and propylparaben. The invention also relates to the process for obtaining the composition.
CN101991597A Applications of oral pharmaceutical composition to preparation of medicament for preventing or treating kidney diseases The invention belongs to the field of medicines, in particular to the applications of an oral pharmaceutical composition to the preparation of a medicament for preventing or treating kidney diseases including diabetic nephropathy and hypertensive nephropathy. The pharmaceutical composition provided by the invention comprises an active ingredient of rosuvastatin or pharmaceutically acceptable salts thereof and heparin, heparin with low molecular weight or pharmaceutically acceptable salts thereof. Proved by experiments on animal, the pharmaceutical composition provided by the invention has favorable prevention and treatment action on the diabetic nephropathy and the hypertensive nephropathy of mice and has favorable synergy. The pharmaceutical composition can be prepared into solid oral preparations including tablets and capsules according to a conventional preparation technology.
WO2004093907A3 Therapeutic agents for treating dermatitis, alopecia and itching and transgenic animals for evaluating such therapeutic agents Using the transgenic mouse, the effect of an agent to be tested on dermatitis for which autoimmune dermatitis is a typical example and/or alopecia and/or itch can be examined, and an agent for preventing / treating dermatitis, alopecia or itch can be provided.
US20110111061 Compositions and Methods for the Treatment of Skeletal Metastatic Lesions and Fractures Compositions and methods for the treatment of fracture and metastatic bone cancer are disclosed.
US20120202892 Cannabinoid-Containing Compositions and Methods for Their Use This invention relates to cannabinoid-containing compositions, particularly cannabinoid-containing gel formulations and methods for the treatment of traumatic injury, e.g., strains, sprains and contusions, and disease conditions, e.g., arthritis, particularly osteoarthritis. The methods involve topically applying a cannabinoid or a cannabinoid-containing composition to a subject's skin near, or distant from, the area of the injury or the area affected by the disease condition, e.g., an arthritic joint. The cannabinoid-containing composition is preferably a pharmaceutically acceptable gel containing a therapeutically effective amount of a cannabinoid sufficient to alleviate the symptoms associate with the injury or disease condition.
EP2149369A1 Instant oral formulations, gelling at room temperature, useful to treat physical wasting and the depressive syndrome associated with cachexia, anorexia, metabolic disorders, endocrine disorders and dysphagia Disclosed are oral formulations containing whey protein, a mixture of tri- and tetrapeptides obtained from hydrolysis of whey protein, and a methyl donor selected from mono-, di- and trimethylglycine and S-adenosyl-methionine.
CN101909633A Use of a gamma-secretase inhibitor for treating cancer The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound, as well as the use of compound (1) for the manufacture of medicaments for treating cancer according to the dosages and schedules specifically disclosed herein.
CN103191439A Silibinin-ursodesoxycholic acid solid dispersoid and preparation method thereof The invention belongs to the technical field of medicine and relates to a silibinin-ursodesoxycholic acid solid dispersoid and a preparation method thereof. In the silibinin-ursodesoxycholic acid solid dispersoid, a mole ratio of silibinin to ursodesoxycholic acid is 1: 0.5-5 and preferably is 1: 0.5-3. The silibinin-ursodesoxycholic acid solid dispersoid is prepared by a solvent method or a grinding method. The drugs in the silibinin-ursodesoxycholic acid solid dispersoid are amorphous. Compared with the raw drugs, the silibinin-ursodesoxycholic acid solid dispersoid has the advantages that a dissolution rate of silibinin in the silibinin-ursodesoxycholic acid solid dispersoid is obviously improved; and after oral administration of the silibinin-ursodesoxycholic acid solid dispersoid by rats, a silibinin in-vivo absorption rate is obviously improved.
US20120079616 Npc1l1 (npc3) and methods of use thereof The present invention provides human, rat and mouse NPC1L1 polypeptides and polynucleotides encoding the polypeptides. Also provided are methods for detecting agonists and antagonists of NPC1L1. Inhibitors of NPC1L1 can be used for inhibiting intestinal cholesterol absorption in a subject.
US20090010935 Compositions and Methods of Treating Tumors Methods of treating an individual who has an erbB protein mediated tumor is disclosed. Methods of preventing erbB protein mediated tumors in an individual are disclosed. The methods comprise administering to the individual a nucleic acid molecule that encodes a protein that dimerizes with an erbB protein and that is deficient in tyrosine kinase activity. Composition that comprise such nucleic acid molecules including pharmaceutical compositions are disclosed.
US20050159365 Hepatits c virus inhibitor comprising alpha-glycosylceramide as the active ingredient This invention provides a growth inhibitor of human hepatitis C virus comprising, as an active ingredient, α-glycosylceramide used for patients infected with the aforementioned viruses. This inhibitor of hepatitis C virus comprises, as an active ingredient, a compound represented by formula (I) or a salt or solvate thereof.
WO2007098504A1 Prodrugs of curcumin analogs The invention provides sulfur-linked and nitrogen-linked peptidic conjugates of curcumin analogs that can provide increased water solubility and photostability as compared to the corresponding unmodified curcumin analogs without sacrificing therapeutic efficacy. The conjugates, which are believed to act as prodrugs, can be used therapeutically in the same manner as the unmodified curcumin analogs, such as in the treatment or prevention of cancer, diabetes, or inflammatory diseases. One conjugate comprises 3,5-Bis-(2-fluorobenzylidene)-piperidin-4-one, or a salt thereof, covalently attached through a sulfur linkage to a thiol-containing peptide such as glutathione.
CN101019832A Docetaxel fat milk and its freeze dried prepn and their prepn process The present invention belongs to the field of medicine technology, and is especially one kind of fat milk connecting docetaxel, its freeze dried preparation and their preparation process. The fat milk contains docetaxel in 0.05-0.2 wt%, oil for injection, emulsifier, stabilizer, isoosmotic regulator, and pH regulator. The fat milk is prepared through adding docetaxel into oil for injection, adding stabilizer and antioxidant through stirring to dissolve docetaxel and obtain the oil phase; dissipating glycerin and emulsifier into water for injection to form the water phase; mixing the water phase and the oil phase to obtain initial emulsion; regulating pH to 5-6 and high pressure homogenizing to obtain the fat milk. The fat milk and its freeze dried preparation have high safety, high stability, less toxic side effect, and high curative effect, and are used for clinical intravenous injection.
CN101879427A Doxorubicin hydrochloride-carrying natural polymer-poly(3-benzene acid acrylamide) composite nanospheres, manufacturing method and application thereof The invention discloses natural polymer-poly(3-benzene acid acrylamide) composite nanospheres. The surfaces of the natural polymer-poly(3-benzene acid acrylamide) composite nanospheres are hydrophilic natural polymers; the interiors are hydrophobic poly(3-benzene acid acrylamide); the number average molecular weight of the natural polymer is in a range of between 2,000 and 100,000; the content ofthe natural polymer is 5 to 70 percent of the mass of the composite nanospheres; the number average molecular weight of the poly(3-benzene acid acrylamide) is in a range of between 1,000 and 10,000; the content of the poly(3-benzene acid acrylamide) is 30 to 95 percent of the mass of the composite nanospheres; and the average grain diameter of the composite nanospheres is of between 40 and 100 nanometers. The composite nanospheres of the invention have the characteristics of high biocompatibility and stable chemical properties. The composite nanospheres of the invention can be used as a medicament carrier, has a sustained-release effect, and can be used as a carrying agent in a boron neutron capture therapy. The invention also discloses a manufacturing method for the composite nanospheres.
US20120024743 Transdermal pharmaceutical preparations The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.
EP1178810B1 Use of bisphosphonic acids for treating angiogenesis A method for the treatment of angiogenesis in a patient in need of such treatment, e.g. a tumour patient or a patient suffering from an inflammatory disease, which comprises administering, preferably via an intra-arterial route, an effective amount of a bisphosphonate, e.g. pamidronic acid or zoledronic acid or salts or hydrates thereof, to the patient.
CA2252084C Cytoprotective compounds The present invention provides compositions and methods for protecting cells from injury due to intrinsic membrane lysis, oxidation and/or invasion by destructive agents. A composition of the formula: (see formula I) wherein A comprise H, OH, a sugar moiety, an ether, an ester, an amide, NH2, or an acid or salt thereof, B is selected from the group consisting of N, NR, P, P=O, CH and CR, wherein R is an alkyl chain of 1 to 6 carbons and the chain may be functionalized or non--functionalized. C1, C2 and C3 are connecting groups which may be different and are selected from the group consisting of -(CH2)n- and (CH2CH2-O)y wherein n is an integer from 1 to 24, -(CH2)n- may be functionalized or non-functionalized, and y is an integer from 1 to 12, and D1 and D2 are fatty acid chains which may be different and are selected from the group consisting of fatty acid esters including CH3(CH2)n COO, and fatty acid amides of the form CH3(CH2)n CONH, wherein n is an integer from 1 to 32, at least one of the fatty chains is unsaturated at one or more positions, and the fatty chains may be of different lengths and may be unsaturated at different locations. Even more particularly, the present invention provides compositions and methods for treating or prophylactically inhibiting phospholipase mediated injury, injury due to oxidation, and inflammation. In a very specific sense, this invention provides compositions and methods of making these compositions that are inhibitors of phospholipase.
WO2011120327A1 Anti-tumor medicament of structure of diarylurea or thiourea kind based on indazole or aza-indazole An anti-tumor medicament, especially an anti-tumor medicament of structure of diarylurea or thiourea kind based on indazole or aza-indazole is disclosed in the present invention. The structure of the medicament is shown as formula (Ia) or (Ib): wherein, Z is N atom or C atom; W is O, S, NH, NOH, NCN and so on; M is O, S, N, CH and so on; n is 1 or 2; Y and R are halogen atom, H, R1, CF3, OCF3, OH, OR2, OCOR3, NH2, NHR4, NR5 2, NHCOR6, carboxyl, ester, cyano, thiol, alkylthio, sulfonyl, sulfoxide group, sulfonic group, sulfonate group, sulphonylamino, keto, aldehyde group, nitro group, nitroso group. The medicament can be used for treating lung cancer, renal carcinoma, colon cancer, liver cancer, stomach cancer and breast cancer in human.
WO2008047831A1 Jak inhibitor Disclosed is a JAK inhibitor or the like containing a nitrogen-containing heterocyclic compound represented by the formula (I) below or a pharmacologically acceptable salt thereof as an active ingredient. [In the formula (I), W represents a nitrogen atom or -CH-; X represents -C(=O)- or -CHR4- (wherein R4 represents a hydrogen atom or the like); R1 represents a group represented by the following formula: (wherein Q1 represents -CR8- (wherein R8 represents a hydrogen atom, a substituted or unsubstituted lower alkyl or the like) or the like; Q2 represents -NR15- (wherein R15 represents a hydrogen atom, a substituted or unsubstituted lower alkyl or the like) or the like; and R5 and R6 may be the same or different and represent a hydrogen atom, a halogen, a carboxy, a substituted or unsubstituted lower alkyl or the like) or the like; and R2 and R3 may be the same or different and represent a hydrogen atom, a halogen, a substituted or unsubstituted lower alkyl or the like.]
WO2006024784A3 Aminoglycoside analogues, uses thereof for treating microbial diseases and synthesis thereof The invention concerns the use of compounds comprising a cyclopentane cycle, substituted in positions (1) and (3) by primary, secondary or tertiary amino groups, identical or different, optionally protected by a protecting group, said amino groups being in cis configuration, for preparing a medicine for treating microbial diseases, such as bacterial infections, viral infections or mycoses.
WO2007065821A1 Propionamide compounds as antiinflammatory agents The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula (I) and pharmaceutical compositions comprising the compounds of formula (I).
US20090275616 Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
US20100151027 Method of treating pain utilizing controlled release oxymorphone pharmaceutical compositions and instruction on dosing for renal impairment The invention pertains to a method of using oxymorphone in the treatment of pain by providing a patient with an oxymorphone dosage form and informing the patient or prescribing physician that the bioavailability of oxymorphone is increased in patients with renal impairment.
US8673894 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
US20080125382 Extracellular superoxide dismutase (EC-SOD) gene delivery to prevent oxidative injury The present invention relates to compositions and methods for preventing oxidative injury to a cell. The compositions comprise a lipid formulation and a recombinant nucleic acid encoding an extracellular superoxide dismutase (EC-SOD), which upon transfection of a target cell is expressed by the cell and acts as an enzymatic antioxidant. The invention also provides for an isolated organ treated with the claimed composition or method.
US20090247593 N-thiazol-2-yl-benzamide derivatives The invention relates to compounds of the formula I wherein the variables are as defined in the claims. The compounds are A2A-receptor ligands, such as antagonists, agonists, reverse agonists or partial agonists, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.
CA2335250C Temperature-sensitive liposomal formulation Temperature sensitive liposomes containing active agents are described. The liposomes comprise phospholipids and a surface active agent, such as a lysolipid, that increases the amount of active agent released by the liposome at the phase transition temperature of the liposome. Such liposomes are useful in methods of administering active agents using mild hyperthermic conditions.
WO2006129859A3 Combinations of a squalene synthase inhibitor and a hmg-coa reductase inhibitor for treating hyperlipidemia A pharmaceutical composition useful for the prevention and/or treatment of hyperlipidemia, which comprises combining an effective amount of a squalene synthase inhibitor and a HMG-CoA reductase inhibitor is provided. Furthermore, a method for preventing and / or treating hepatic toxicity caused by the administration of a HM6-C0A veductase inhibitor, which comprisis adminisvering an effective amount of a sgualence synthase inhibitor, is provided .
US20100317638 Neuroactive 13,24-Cyclo-18,21-Dinorcholanes and Structurally Related Pentacylic Steroids Novel pentacyclic steroids and pentacyclic D-homosteroids comprising: (i) the tetracyclic steroid ring system or tetracyclic D-homosteroid ring system, respectively; (ii) a C(3) substituent selected from the group consisting of (a) a hydroxyl or carboxyl in the α-configuration and (b) a sulfate or other negatively charged moiety; and (iii) a fused fifth ring, the fused fifth ring comprising a hydrogen bond acceptor, and (a) in the case of the pentacyclic steroid the C(13) and C(17) carbons, or (b) in the case of the pentacyclic D-homosteroid the C(13) and C(17a) carbons, having utility as anesthetics and in the treatment of disorders relating to GABA function and activity.
CA2273922C Novel saponin compositions and uses thereof The present invention is in the field of medicinal chemistry. In particular, the invention is related to vaccines comprising novel combinations of saponin adjuvants, to pharmaceutical compositions and vaccines comprising these novel combinations, to methods of using these novel combinations to enhance the immune response of an individual to an antigen, and to the use of the novel combinations to increase the immunogenicity of vaccines.
CN102836170A Hyperoxia compound glycine pyridoxal electrolyte injecta The invention discloses hyperoxia compound glycine pyridoxal electrolyte injecta which contains high-concentration dissolved oxygen, electrolyte, mannitol and piracetam. After intravenous infusion, the hyperoxia compound glycine pyridoxal electrolyte injecta can not only play a conventional role of dehydration, but also notably improve oxygen content of blood, replenish loss of the electrolyte caused by the dehydration, play important roles in lightening electrolyte disturbance and protecting important viscera from anoxia damage, and be safely and widely used to cure encephaledema, reduce intracranial pressure and intraocular pressure, effectively reduces occurrence rates of various complications, and has good double functions of cerebral protection. A plurality of kinds of effective composite ingredients contained by the hyperoxia compound glycine pyridoxal electrolyte injecta respectively reduce working concentration and working dosage of single drug. The hyperoxia compound glycine pyridoxal electrolyte injecta greatly reduces injection pains and renal toxicity, overcomes three big difficult problems that mannitol is crystallized below 15 DEG C and the like, is favorable for being used for emergency treatment at different environment temperatures, and has rather important clinical application values, and wide social and economic benefits.
EP2787002A1 Oleanolic acid amidate derivatives, preparation methods and uses thereof The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel amidated derivatives of oleanolic acid according to formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
WO2007073005A1 Regulator of methyl transfer reaction Disclosed are: a regulator of the methylation of a biological polymer, wherein the regulator comprises carbon monooxide; a method for regulating the methylation of a biological polymer; an inducer of the differentiation of a cell; and a method for inducing the differentiation of a cell.
CN101804064A Application of dihydroquercetin and glucoside compounds to preparing drug-resistance bacteria medicine The invention discloses application of dihydroquercetin and glucoside compounds to preparing a medicine for resisting drug-fast bacteria. With the invention, the dihydroquercetin and glucoside compounds can be extracted from decogenus plants, such as hypericum japonicum Thunb, and the activity of the dihydroquercetin and glucoside compounds for resisting the drug-fast bacteria can be proved; proved by a pharmacological experiment, the dihydroquercetin and glucoside compounds not only have remarkable direct inhibition function on common-clinically meticillin-resistant staphylococcus aureus (MRSA), but also can enhance the action of the traditional antibiotic for resisting the drug-fast bacteria. The dihydroquercetin and glucoside compounds can be further used as active components and used for preparing a medicine for treating the drug-fast bacteria infection; and preparation forms includes oral preparations, injections and/or external preparations which are prepared by combining with acceptable carriers.
US20060234342 Human DNA topoisomerase I alpha Disclosed is a human is a hTopI-α polypeptide and DNA (RNA) encoding such hTopI-α polypeptide. Also provided is a procedure for producing such polypeptide by recombinant techniques and antibodies and antagonists against such polypeptide. Also provided are methods of using the antibodies and antagonist inhibitors to inhibit the action of hTopI-α for therapeutic purposes such as an antitumor agent, to detect an autoimmune disease, or retroviral infections and to treat adenocarcinoma of the colon. Diagnostic methods for detecting mutations in the coding sequence and alterations in the concentration of the polypeptides in a sample derived from a host are also disclosed.
US7294718 Synthesis of a 4-methylthiazole-4(S)-carboxylic acid compound Benzimidates can be reacted with a large number of nucleophiles, leading to a wide variety of products. The present invention discloses a facile synthesis for ethyl 2,4-dihydroxybenzimidate, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid or 2,4-dibenzyloxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.
CN101518510A Method for preparing tanshinone micelle The invention relates to a method for preparing tanshinone micelle, which is characterized by comprising the following raw materials according to the parts by weight: 0.01-50 of tanshinone, 0.01-50 of surface active agent, 0.01-50 of cosurfactant and the balanced deionized water. The invention has the advantages that the obtained tanshinone micelle has an average particle diameter below 10 nm, good dispersion, stable nature and convenient preparation, is transparent and Turkey red, and can solve the problem of insolubility of tanshinone extractive in water and provide a preference for the development of tanshinone liquid products.
US20060172019 Cannabinoid receptor inverse agonists and neutral antagonists as therapeutic agents for the treatment of bone disorders The present invention pertains to cannabinoid (CB) receptor inverse agonists and neutral antagonists, and especially CB1 and CB2 inverse agonists and neutral antagonists; such as, for example, certain pyrazole compounds; their use in the inhibition of osteoclasts (for example, the inhibition of the survival, formation, and/or activity of osteoclasts), and/or in the inhibition of bone resorption; their use in connection with treatment of bone disorders, such as conditions mediated by osteoclasts (e.g., increased osteoclast activity) and/or characterised by (e.g., increased) bone resorption, such as osteoporosis (e.g., osteoporosis not associated with inflammation; e.g., osteoporosis associated with a genetic predisposition, sex hormone deficiency, or ageing), cancer associated bone disease, and Paget's disease of bone.
WO2010045013A1 Phenyl substituted thieno [2,3-d] pyrimidines and their use as adenosine a2a receptor antagonists This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein R1 and R2 are definedin the specification. Disorders treated and/or prevented include Parkinson's Disease.
CN101698673A Prawn white spot syndrome virus VP37p polypeptide fragment and application thereof The invention utilizes prawn white spot syndrome virus (WSSV) gene expression technology to obtain a segment which is coded by a prawn white spot bacilliform virus WSV254 gene and is named as VP37p. The invention also relates to a method for manufacturing the VP37p, application of polynucleotide and polypeptide of the VP37p, and an antibody specifically bound with the polypeptide of the VP37p. The invention identifies the function of the VP37p through a biological method for the first time; the VP37p is one of WSSV attachment protein fragments; and the inhibition on the gene and expression products thereof may be one of effective ways of preventing and controlling prawn white spot disease and expects to be applied to the prevention and control of the prawn white spot disease.
EP2291084A1 Carbonate prodrugs and methods of using the same The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.
CN102504267A Paclitaxel bonded amphipathic aliphatic polyester-b-polyphosphate high polymer and preparation thereof The invention belongs to the field of medicament control release, and in particular relates to a paclitaxel bonded amphipathic aliphatic polyester-b-polyphosphate high polymer. The high polymer comprises a polyphosphate chain segment, an aliphatic polyester chain segment and a paclitaxel group, wherein the two ends of the aliphatic polyester chain segment are respectively connected with the paclitaxel group and the polyphosphate chain segment by virtue of ester bonds; the aliphatic polyester chain segment is selected from a poly(epsilon-caprolactone) chain segment or a polyactic acid segment. The high polymer can perform self-assembly in a phosphoric acid buffer solution PBS to form a hydrophobic medicament and a micelle in which lipophilic aliphatic polyester is used as a core and water-soluble polyphosphate is used as a shell. Through the preparation, on one hand, the strong hydrophobicity of a paclitaxel medicament is improved so as to avoid the rejection reaction of the medicament in the in vivo transportation process, and on the other hand, the medicament is slowly released through degradation of polyester so as to avoid the harmfulness of sharp increase of medicament concentration on other normal cells of tissue organs, thereby reaching the effect that an anti-tumor medicament is released controllably.
US20100216779 Imidazopyridine Kinase Inhibitors The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
US7612047 Degradation-resistant mononucleoside phosphate compounds The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.
US7098209 Phosphodiesterase inhibitors; cardiovascular disorders; erectile dysfunction; hypotensive agents; respiratory system diosrders; chronic obstructive pulmonary disease; congestive heart failure; antihistamines; antiallergens Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as thereapeutic agents. In particular, the invention relates to compounds that are potent and selective inhibitors of cyclic guanosine 3′, 5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5, and have utility in a variety of therapeutic areas wherein such inhibition is considered beneficial, including the treatment of cardiovascular disorders and erectile dysfunction
US7704960 Administering Erythromycin A having had the cladinose moiety in the 3-position removed by acidolysis to produce an antiinflammatory agent having no antibiotic properties; chronic respiratory system disorders; cytokine suppressive antiinflammatory drugs; antiarthritic agents; antiischemic agents Macrolide compounds endowed with antiinflammatory activity are described, and more particularly macrolide derivatives lacking cladinose in position 3, with antiinflammatory activity, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing them as active ingredient.
WO2009085198A3 Combination of metformin r-(+)-lipoate and antiobesity agents for the treatment of diabetic hyperglycemia and diabetic complications Disclosed are pharmaceutical compositions, methods of treatment, and kits for the treatment of Type 2 diabetic hyperglycemia and diabetic complications using combination treatments comprising metformin R-(+)-lipoate and antiobesity agents.
CN1579418A Preparation pixuanjing for treating psoriasis and its preparation method The invention belongs to medical medicine producing field, especially relates to an external medicine for curing skin shallow fungus disease. The ringworm of the body, tinea cruris, tinea on manus and pedes are diseases which are difficult to be cured, the product is psoriasis cleaner for curing shallow fungus diseases. It is made up of salicylic acid, benzoic acid, boracic acid, bromo geramine, alcohol. The merits of the invention are: it is colorless transparent liquid, convenient, and it can increase the compliance of patient, it will not contaminate the cloths, and it has functions of bacteria, fungus, virus sterilization, it can relieve itching, diminish inflammation, and relieves symptom. The process is simple, the cost is low, and it has double functions of fungus resisting and bacteria resisting.
US20110092598 Driectly Compressible High Functionality Granular Microcrystalline Cellulose Based Excipient, Manufacturing Process and Use Thereof An improved excipient comprising substantially homogeneous particles of a compressible, high functionality granular microcrystalline cellulose based excipient is provided. The improved excipient comprises microcrystalline cellulose, a binder and a disintegrant, and is formed by spraying a homogeneous slurry of the components. The excipient provides enhanced flowability/good flow properties, excellent/high compactibility, and increased API loading and blendability as compared to the individual components, and as compared to conventional excipients formed from the same materials. The improved excipient has strong intraparticle bonding bridges between the components, resulting in a unique structural morphology including significant open structures or hollow pores. The presence of these pores provides a surface roughness that is the ideal environment for improved blending with an API.
CN102863472A Combretastatin A-4 analogue, preparation method of combretastatin A-4 analogue and application of combretastatin A-4 analogue in preparing anti-tumor drugs The invention provides a combretastatin A-4 analogue. The structure of the combretastatin A-4 analogue is represented by general formula (I), wherein R1 represents -H, OH or a metal phosphate substituent group, R2 represents -OH or the metal phosphate substituent group, and the metal phosphate substituent group is -OP(O)(ONa)2, -OP(O)(OK)2, -OP(O)(OLi)2, -OP(O) O2Zn or -OP(O) O2Ca. A pharmacology experiment shows that the combretastatin A-4 analogue can inhibit polymerization of endothelial cell tubulin, damage forming of lumens and lead to tumour organization center necrosis, and the combretastatin A-4 analogue can be applied in anti-solid tumor drugs or in tumor vessel breakers and is wide in application prospects.
US20090053263 Inhibitors of Enveloped Virus Infectivity The present invention relates to treatment of infection by enveloped viruses through the use of papain-like cysteine protease inhibitors and kits thereof. Specifically, methods for treatment of filoviruses as well as other enveloped viruses such as Nipah, in particular using cathepsin inhibitors are described.
CN102058579A Application of dehydrocostuslactone to preparing drug for inhibiting angiogenesis The invention relates to application of dehydrocostuslactone to preparing a drug for inhibiting angiogenesis. The invention has the advantages of providing the novel application of the dehydrocostuslactone, finding the anti-angiogenesis of the dehydrocostuslactone for the first time, finding that the dehydrocostuslactone can effectively inhibit the multiplication, the migration and the canaliculization of vascular endothelial cells for the first time, showing that the dehydrocostuslactone has the activity of the anti-angiogenesis and can be used as an angiogenesis inhibitor as well as can be used as the angiogenesis inhibitor used for preparing the angiogenesis drug and treating vascularization dependent and vascularization relevant diseases of tumors, arthritis, parapsoriasis guttata, eye disorders, atherosclerosis and the like.
EP0815100B1 Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of formula (1.0) to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds wherein X is N, C or OH and R is (I) or (II) are disclosed.
WO2006043858A3 Method for cleaning the internal environment of an organism and endoecological correction agent The invention relates to medicine, in particular to methods and means for removing toxic substances and harmful waste products from the internal environment of an organism and can be used for preventing and correcting functional disorders and diseases caused by the action of environmental exhausting factors on an organism. Said invention makes it possible to develop a pluripotential method for cleaning the internal environment of an organism and an agent for carrying out said method which is based on a vegetable raw material, vitamins and microelements and takes into account all elements for an endoecological homeostasis maintaining system. The inventive method for cleaning the internal environment of an organism consists in activating the functions of a natural system for cleaning a human organism by simultaneously stimulating all basic organism internal environment cleaning mechanisms: intercellular environment excretory cleaning, endocellular biotransformation of xenobiotics and antioxidant protection, wherein an integrated endoecological correction agent is orally administrated. An inventive three-complex endoecological correction agent containing medicinal plants, vegetable extracts and natural antioxidants is also disclosed.
EP1216246B1 N-substituted 4-aminopteridines, synthesis and use thereof as pharmaceutical agent Compounds of formula (I), where preferably: A = a bridge of partial formula (II) or (III), R?1 and R2¿ = independently (substituted) alkyl, aryl or aralkyl, or together form a heterocycle, R3 = H, -CO-Alkyl, or -CO-Aryl, R4 = Aryl,-CO-O-Aryl or -CO-Aryl and R5 = H, are potent inhibitors of NO-synthase and are suitable as pharmaceutical agents for prophylaxis and treatment of disease states associated with a disturbed NO metabolism.
US20070287722 Drop Preparations Comprising Dimetindene The invention relates to orally administered drops comprising the pharmaceutically active substance dimetindene, which drops are sorbitol-free and ethanol-free and characterized by special, very beneficial properties regarding physical and chemical stability, organoleptic properties as well as suitability for children.
US20100284994 Use of edta and its derivatives for prevention and treatment of bacterial intestinal diseases of pigs and for increasing the effects of antibiotics exerted in such diseases The invention relates to the use of ethylenediamine tetraacetic acid (EDTA) and its derivatives, i.e. its salts and complexes for prevention and treatment of bacterial intestinal diseases of pigs and for increasing the effects of antibiotics exerted in such diseases. The invention also relates to compositions for animal husbandry, i.e. to veterinary compositions and to feeds and drinks which can be consumed by pigs, comprising EDTA or its derivatives.
US20050239054 Drug screening compounds having esterified phosphonate or carboxyl groups with novel enzyme GS-7340 Ester Hydrolase and identifying the compound as a suitable prodrug by the formation of a phosphonic acid or carboxylic acid; candidate compounds Methods are provided for identifying anti-HIV therapeutic compounds substituted with carboxyl ester or phosphonate ester groups. Libraries of such compounds are screened optionally using the novel enzyme GS-7340 Ester Hydrolase. Compositions and methods relating to GS-7340 Ester Hydrolase also are provided.
CN101239187B Functionalization carbon nano-tube for tumor lympha targeted therapeutic carrier The present invention relates to a new carrier for target treating tumour lymph which belongs to molecular biology medicine manufacturing field, specific concerned with a initiative targeting new carrier-functionalization carbon nano-tube for treating tumour lymph, and a method for preparing the same. The functionalization modified carbon nano-tube with corresponded particle size is prepared by detecting the size of tumour lymphatic capillaries gap and window hole, and absorbs specific medicine, carries into tumour lymph system then release it. It is proved by experiment that said functionalization carbon nano-tube absorbed with medicine has better desorbing function in lymph system and blood plasma, and better lymph tendency, also can reach availability density for kill tumour with better chemo-treatment effect of lymph.
WO2012045906A1 Polyhydroxylated aminocyclohexanes and use thereof for treating lysosomal diseases The invention relates to polyhydroxylated aminocyclohexane compounds and to the use thereof for treating lysosomal diseases such as Gaucher's disease. The invention also relates to the method for the synthesis of said compounds.
WO2007088041A1 Compounds for the inhibition of integrins and use thereof The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring., Ar is either absent or phenylene; Ψ is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
CN103054879A Norethisterone acetate-containing compound estradiol transdermal sustained release preparation and preparation method thereof The invention discloses a norethisterone acetate-containing compound estradiol transdermal sustained release preparation and a preparation method thereof. The preparation comprises a backing layer, a protective film and a frame layer between the backing layer and the protective film, wherein the frame layer comprises an upper frame layer, a lower frame layer and a controlled release film between the upper frame layer and the lower frame layer; and the backing layer covers the surface of the lower frame layer. The upper and lower frame layers are respectively wrapped by estradiol and norethisterone acetate in a certain ratio, an intermediate frame layer is wrapped by a special transdermal patch of the controlled release film, estrogen estradiol effects in relieving or eliminating climacteric syndromes and preventing osteoporosis are fully played, and the preparation also has the characteristics of small stimulus to human bodies, small side effects, quality stability and long effective time.
WO2011064274A1 Use of h3 histaminergic agonists for the treatment of addiction to drugs of abuse The present invention relates to H3 histaminergic agonists, compositions thereof, and methods for treating or preventing addiction to drugs of abuse in a subject. The methods comprise administering to a subject in need thereof an effective amount of one or more H3 histaminergic agonists to prevent addiction, diminish the voluntary seeking of drugs of abuse, facilitate the cessation of the addictive behavior, and to prevent relapse.
US20120321704 Compound sea Cucumber Product, Preparation Method, and Dosage Forms Thereof A compound sea cucumber product, preparation method thereof and dosage forms thereof are disclosed. A fresh sea cucumber is cut open, the viscus thereof is taken out, and they are well-cleaned respectively and put into an airtight container; at 70˜130° C., gelatinate for 1 min˜20 hours; thereafter freeze-dry till the water content is less than 10 wt %; apply coarse crushing till the fineness reaches 10˜300 mesh; then apply ultra-micro crushing by means of an airflow crusher until the fineness reaches 100˜3000 mesh; lastly apply nanometer crushing by means of high-energy ball grinding mill till the fineness reaches 10˜1000 nm. The nanometer sea cucumber extract is mixed with panax pseudo-ginseng saponins extract at the proportion of 99˜80 wt %:1˜20 wt %. The compound preparation of nanometer sea cucumber and panax pseudo-ginseng saponins can greatly enhance the pharmacological functions of the sea cucumber single preparation or the panax pseudo-ginseng single preparation and eliminate the side effects of the single preparations when used alone. The compound preparation can achieve a better health-care effect than the single preparations and it can be applied for various health-care and medicinal purposes.
WO2005033099A3 Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof The present invention relates to novel dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula (I), and their analogs, isomers, pharmaceutical compositions and therapeutic uses, methods of making the same.
CN103222981A Application of dendrobium candidum polysaccharide in preparing drug for promoting hair growth The invention relates to application of dendrobium candidum polysaccharide in preparing a drug for promoting hair growth, wherein the dendrobium candidum polysaccharide in the drug is 0.1%-5% by weight. The dendrobium candidum polysaccharide in the drug disclosed by the invention can be used for regulating up expression of a vascular endothelial growth factor (VEGF) gene in a keratoderma forming cell (HaCaT cell) blood vessel, so that the effect of prompting the hair growth is achieved.
CN103656652A Dual-sensing response type polymer nano-micelle as well as preparation method and application thereof The embodiment of the invention provides a dual-sensing response type polymer nano-micelle. The component of the nano-micelle is n-butylamine-polylysine (folic acid/2,3-dimethylmaleic anhydride)-b-polycysteine, wherein n-butylamine is connected with one end of a polylysine chain segment through an amido bond, and the other end of the polylysine chain segment is connected with a polycysteine chain segment; folic acid is connected with the amidogen of the side chain part of the polylysine chain segment through the amido bond; 2,3-dimethylmaleic anhydride is connected with the rest amidogen of the side chain of the polylysine chain segment in an amido bond manner. The dual-sensing response type polymer nano-micelle can be used as a carrier of a hydrophobic drug, is biodegradable and stable in property, has a function of positive target transfer, and can realize charge reversal and reducing response. The embodiment of the invention also provides a preparation method and application of the dual-sensing response type polymer nano-micelle.
CN102448955A Amino pyrimidine anticancer compounds Compounds of Formula (1), as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
US20120135981 Novel substituted triazole and imidazole derivatives as gamma secretase modulators The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
CN103463124A Bacterial cellulose/chitosan composite gel and preparation thereof, and application of composite gel in body surface wound surface healing The invention relates to a bacterial cellulose/chitosan composite gel and preparation thereof, and application of the composite gel in body surface wound surface healing. The composite gel is composed of a chitosan solution, bacterial cellulose, an antimicrobial agent, a thickener solution and a neutralization agent. The invention also relates to application of the bacterial cellulose/chitosan composite gel in preparing body surface wound surface healing medicines. The preparation method comprises the following steps: uniformly mixing the chitosan solution, thickener solution, bacterial cellulose and antimicrobial agent, adding the neutralization agent to regulate the pH value to 6.0-9.0, and standing for deforming. The composite gel provided by the invention has favorable film-forming action, and performs the functions of isolating the wound surface and protecting the wound; and the bacterial cellulose/chitosan has the advantages of simple preparation process and easy technical control, and is convenient for industrial production.
WO2013093095A1 Bisarylsulfonamides useful in the treatment of inflammation and cancer A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
CN1895565A Preparation of turtle essence oral liquid An oral liquid of turtle extract for improving immunity and increasing the resistance of human body is prepared from turtle and multiple noble Chinese-medicinal materials through unique process.
US7658917 A beta aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural beta amyloid peptides when contacted with the peptides. Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural β amyloid peptides (β-AP). In a preferred embodiment, the β amyloid modulator compounds of the invention are comprised of an Aβ aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural β amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural β-AP aggregation when the natural β-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
EP1781665A2 Olanzapine salts and their conversion to olanzapine free base The present invention provides salts olanzapine useful as intermediates in the isolation of olanzapine from complex reaction mixtures. These salts can be used for the production of olanzapine base which has a suitable purity for pharmaceutical use and can easily be converted to anhydrous olanzapine polymorphic form I, in high yields.
US20090270506 Crystalline structure of oxidosqualene synthase The present invention relates to crystal forms of mammalian OSC and the crystal structure information obtained from them, to methods of preparing such crystal forms, and to their use for the identification and/or design of inhibitors of OSC activity. A further subject matter of the invention are methods for the identification and/or design of inhibitor compounds of OSC activity, the inhibitor compounds of OSC activity identified by these methods and their use in pharmaceutical compositions for the treatment and/or prevention of diseases which are associated with OSC comprising hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections and gallstones, and/or treatment and/or prophylaxis of impaired glucose tolerance, diabetes, tumors and/or hyperproliferative disorders, preferably for the treatment and/or prophylaxis of hypercholesterolemia and/or hyperlipemia.
CN101229283A Zhongganling capsule and preparing method thereof The invention discloses a medicine of a bad cold capsule and a preparation method thereof; the invention takes pubescent holly, notopterygium, kudzu root, gypsum, vervain, isatis root, artemisia, chlorpheniramine and analgin as raw materials; decoct solutions which are combined according to different properties of plant medicine, natural medicines and western medicine are filtered and concentrated into dry ointment powders, and granules which are prepared reasonably and scientifically according to proportions after the pretreatment of dry crushing, crushing and power extracting are filled into granule capsules. The invention is unique in formula and preparation method and has exact curative effect and marked efficacy with clinical application.
CN103006681A Compound emulsifiable paste for treating acne and preparation method thereof The invention relates to a compound emulsifiable paste for treating acne and a preparation method thereof. The compound emulsifiable paste comprises the following ingredients by weight percent: 1% of clindamycin hydrochloride, 0.8% of metronidazole, 7%-16% of albolene, 4%-12% of glycerol, 1%-3% of liquid paraffin, 4%-6% of simethicone, 3%-8% of emulsifying agent, 4%-6% of penetration enhancer and the balance of distilled water. The compound emulsifiable paste solves the difficulties that indissolvable drug can not be distributed uniformly, the drug with heat instability is decomposed and subjected to color change when being heated, the possibility of paste preparation in normal temperature can be realized, and the paste is ideal in appearance and is stable. Meanwhile, according to the compound emulsifiable paste, the permeability of corneum of the skin is improved, the effective dose of the drug achieving the wound part is ensured, the bioavailability of effective ingredients of the drug can be improved, the effective dose is reduced, and the toxicity and the skin irritation are low.
CN102000137A Compound catechu capsules and production process The invention discloses compound catechu capsules and a production process. The capsule consists of the following components in parts by weight: 250 parts of catechu, 5 parts of vitamin B2, and 2.5 parts of nicotinic acid. The production process comprises the following steps: (1) crushing and drying; (2) screening; (3) inspecting; (4) totally mixing; (5) inspecting an intermediate product; (6) filling and polishing; and (7) plate pressing. The invention has the effects that: compared with the similar products for treating gastrosis, the compound catechu capsules have the characteristic of strong specificity, has accurate curative effect for gastrosis and duodenal ulcer, but other products do not have remarkable curative effect, and certain chemical medicaments have more side effects to human bodies, so in terms of the curative effect and the side effects, the compound catechu capsules have incomparable advantages compared with the similar products.
CN103083355A Compound sodium chloride injection and preparation method thereof The invention relates to a compound sodium chloride injection and a preparation method of the compound sodium chloride injection. The injection comprises the following components in percentage by weight: sodium chloride, potassium chloride, calcium chloride and sodium hydrogen sulfite. The compound sodium chloride injection provided by the invention has excellent stability which is higher than the stability in the prior art.
WO2011127643A1 Pyridone derivatives The present invention discloses phenylpyridone derivative compounds. The compounds act as a melanin concentrating hormone receptor antagonists, and can be used in preventing, treating or acting as a remedial agent for various circular system diseases, nervous system diseases, metabolic diseases, genital diseases, respiratory diseases and digestive diseases.
CN102924460A 4H-pyrrolo[1, 2-a] benzimidazole derivative and synthesizing method and application thereof Provided are a 4H-pyrrolo[1, 2-a] benzimidazole derivative and a synthesizing method and application of the derivative serving as a fungistat. R1 in a formula represents cyano or normal-butyl, R2 represents cyano or acylamino, and R3 and R4 represent hydrogen, cyano or ester group. A compound of the derivative has remarkable inbibitional effects on various bacteria including escherichia coli, staphylococcus aureus, bacillus subtilis, pseudomonas aeruginosa and the like and can serve as a fungistat, and the minimal inhibitory concentration can reach to 12.5 mug/mL.
CN102698113A Bone reunion powder with sorghum leaf sheath interior wax as sovereign drug The invention discloses a bone reunion powder which takes sorghum leaf sheath interior wax as sovereign drug, has effects in stopping bleeding, removing blood stasis, reuniting bone and promoting granulation; and combines with Radix Notoginseng, Radix Dipsaci and Pulvis Talci to formulate into powder. The powder can be orally administered with yellow wine or baby's urine; or prepared into cataplasm with Herba Cephalanoploris juice for topical dressing. In combination with bone manual reduction and small splint fixation, the powder has good curative effect on normal fracture and hemorrhage type fracture.
CA2615860A1 Thiocolchicoside analogues with myorelaxant and anti-inflammatory activity The present invention relates to 3-demethoxy-3-aminothiocolchicine glycosyl derivatives of general formula (I) in which R is hydrogen, methyl or hydroxymethyl. The compounds of formula (I) have myorelaxant and anti-inflammatory activity.
CN102697747A Dispersible tablet of cefuroxime axetil The invention provides a dispersible tablet of cefuroxime axetil, wherein the preparation formula includes cefuroxime axetil, loading agents, flow aid, disintegrating agents, surface-active agents, flavoring agents, lubricant, essence, and coating powder. According to the invention, specific disintegrating agents are adopted, meanwhile, the use amount of the disintegrating agents is not increased, the dispersion time of the dispersible tablet is shortened, and the dissolution rate of the dispersible tablet is improved; and meanwhile, flavoring agents and essence are added in the formula to mask bitter of the dispersible tablet of cefuroxime axetil, so that the mouth feel of a patient taking the dispersible tablet of cefuroxime axetil can be improved.
US20100047366 Articles with antibacterial and antifungal activity The present invention relates to articles with antibacterial and antifungal activity, comprising zinc sulphide. The yarns, fibres, filaments and articles according to the present invention may be used especially in the manufacture of any product liable to be placed in contact with bacteria and/or fungi, for instance clothing, rugs, curtains, bedclothes and medical textile materials. The present invention also relates to the use of zinc sulphide for manufacturing yarns, fibres, filaments and/or articles with antibacterial and antifungal properties.
CN101190025A Food for sobering-up, promoting digestion and protecting liver The invention relates to the field of health products, in particular to a foodstuff having the functions of antialcoholism, stomach strengthening and liver protection, which solves the problems that the existing medicament for alcoholism has weak alleviation effect, complex process, greater pain, disadvantage that the medicament does not have abvious protection function to the stomach and the liver at the time of sobering up, etc. The foodstuff comprises 0.35-2.80 weight portions of glutamine and 0.35-2.80 weight portions of alanine and has nutritive value, convenient taking and good taste, which can alleviate a hangover, promoting digestion and protect liver.
CN101371839B Novel use of bisbenzylisoquinoline alkaloids The invention discloses a new application of bisbenzylisoquinoline alkaloid. The invention refers to the application of bisbenzylisoquinoline alkaloid, as shown in a formula (I), or pharmaceutically acceptable salt thereof in the preparation of medicament for inhibiting the proliferation of eukaryote tumor cells and medicament for preventing and/or treating tumor. Bisbenzylisoquinoline alkaloid as shown in the formula (I) and the pharmaceutically acceptable salts thereof can combine with G-quadruplex DNA to increase the stability of G-quadruplex DNA, so as to competitively inhibit the combination of a telomerase and a telomere, restrain the activity of the telomerase, weaken the proliferation capability of cells of the telomerase, control the extension of the telomere and accelerate the apoptosis of telomere cells. Vitro cancer cell proliferation experiments prove that: bisbenzylisoquinoline alkaloid has comparatively good inhibition effect on human leukemia cell system HL-60, human gastric cancer cell system BGC-823, human liver cancer system Bel-7402 and human nasopharyngeal cancer system KB, and the inhibition rate to the cancer cells can reach over 90 percent when the medical concentration of bisbenzylisoquinoline alkaloid is higher than 25muM.
CN103254086A Aromatic ester 5-LOX and mPGES-1 inhibitor and application The invention discloses an aromatic ester compound which is used as a double-function inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin E synthetase (mPGES-1), and the compound has the structure shown in the formula III, wherein, R1 and R2 represent hydrogen and nitro or carboxyl respectively. R3, R4 and R5 represent hydrogen, phenyl, C1-C3 alkyl or halogen respectively, or R4 and R3 or R5 form a ring, thereby representing 1,3-butadiene subunit in combination. The external and whole blood enzyme activity test of the compound for 5-LOX and mPGES-1 confirms that the compound has the double-function inhibition activity for 5-lipoxygenase and prostaglandin E synthetase, and can be used for preparing medicaments for treating and preventing various inflammations.
CN103435574A Mercapto benzothiazole substituent acenaphtho-heterocycle compound and application thereof The invention relates to an anti-tumor mercapto benzothiazole substituent acenaphtho-heterocycle compound and application thereof and belongs to the bioorganic field. The compound is characterized in that mercapto benzothiazole is introduced onto acenaphthequinone in a 'nonnaphtho' manner, so that the mercapto benzothiazole substituent acenaphtho-heterocycle compound is designed and synthesized. The conjugation area of acenaphthequinone is increased through benzocyclobutene, the variety of acenaphtho-heterocycle derivatives is expanded, the biological activity of molecule is improved, and the compound has wide anti-tumor activity and can better inhibit the normal growth of various tumor cells with different tissue sources such as cervical cancer, liver cancer and breast cancer.
EP1835895A2 Use of certain phenyl-naphthyl compounds that do not have significant affintiy to er alpha or beta for protection of neurons and oligodendrocytes in the treatment of multiple sclerosis The invention provides a new use for certain SERM-like phenylnaphthyl compounds that do not exhibit affinity for alpha or beta type estrogen receptors (ER) in the treatment of multiple sclerosis.
CN1714785A Concentrated emulsifier containing taxol compound and its using method The concentrated emulsifier containing taxol compound consists of phosphatide in 5-7.5 wt%, surfactant with HLB not lower than 10 in 0-50 wt%, propylene glycol and/or polyvinyl diol in 0-50 wt%, taxol compound or its derivative in 0-40 wt%, where, the polyvinyl diol has average molecular weight of 200-4000. The concentrated emulsifier contains no Cremophor EL, and has non-toxic organic solvent and surfactant adopted. When used, the concentrated emulsifier is first injected into lipid emulsion to make the main component taxol embedded into oil kernel and form emulsion containing taxol for injection.
US20060025471 Xanthenyl cubane analogs with activity at the metabotropic glutamate receptors The present invention relates to therapeutically active cubane compounds, a method of preparing the same, and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating and preventing diseases of the central nervous system related to the metabotropic glutamate receptor system.
CN103637980A Preparation method for promethazine hydrochloride injection The invention belongs to the technical field of medicinal preparations, and specifically relates to a preparation method for a promethazine hydrochloride injection. The preparation method comprises: taking 50-80 mL of injection water, adding 0.05-1 g of an anti-oxidant and stirring for dissolving, then adding 1-4 g of promethazine hydrochloride and stirring for dissolving, continuing to add 0.4-0.8 g of an osmotic pressure conditioning agent and stirring for dissolving, adjusting solution pH to 4-5.5 by a proper amount of a pH conditioning agent, adding injection water to enable the volume of the solution to be 100 mL, filtering, embedding and disinfecting. The prepared promethazine hydrochloride injection is good in stability; through long-time observation on reserved samples, the injection is basically stable in promethazine hydrochloride content, free of deterioration phenomenon during storage and long in validity period; and the injection has the advantage of high biological availability and the like.
US8765713 Method for determination of sensitivity to anti-cancer agent A marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker, wherein the marker for determining sensitivity to an anti-cancer agent is a protein or a fragment, where in the protein or a fragment thereof exhibits a peak at m/z of 5,300 to 5,400, a peak at m/z of 6,130 to 6,230, a peak at m/z of 7,000 to 7,080 a peak at m/z of 7,840 to 7,920, a peak at m/z of 8,920 to 9,000, a peak at m/z of 12,440 to 12,560, a peak at m/z of 17,100 to 17,270, a peak at m/z of 18,290 to 18,470, a peak at m/z of 24,660 to 24,750, a peak at m/z of 35,980 to 36,290, a peak at m/z of 8,650 to 8,750, a peak at m/z of 9,100 to 9,200, a peak at m/z of 11,760 to 11,890, the peaks being determined by means of a mass spectrometer.
EP1654210B1 Stilbene derivatives and their use in medicaments The invention relates to stilbene derivatives of general formula (I), in which at least four of the substituents R1 to R6 do not represent hydrogen. The substituents are effective radical captors, anti-tumour active ingredients and selective cyclooxygenase-2 inhibitors.
CN101550103A 1, 2, 3, 4-tetrahydroisoquinoline derivatives and synthetic method and uses thereof 1, 2, 3, 4-tetrahydroisoquinoline derivatives and synthetic method and uses thereof, the present invention belongs to medicine synthesis technique field, relating to general formula (1) is: X=(CH[2]) [n], n=1-15 or X=CO (CH[2]) [n-1], n=1-15; R[1], R[3], R[4], R[5], R[6] are 1, 2, 3, 4-tetrahydroisoquinoline compounds with different substituents and salt thereof, method thereof and application if medicine. The present invention discloses chemical structure and synthetic method and vitro acetylcholine esterase repress activity of the chemical compounds, which can be developed into new patern medicine for treating alzheimer's disease in further.
US20100240670 4-[(arylmethyl)aminomethyl]piperidine derivatives, their preparation and their therapeutic application The invention relates to 4-[(arylmethyl)aminomethyl]piperidine derivatives of general formula (I) in the form of a base or an addition salt with an acid, and also in the form of a hydrate or solvate, and their preparation process and therapeutic application.
US7501412 e.g. 4-(1-(2-hydroxyethyl)piperidin-4-yl)-2H-isoquinolin-1-one; poly(ADP-ribose)polymerase inhibitor; nicotinamide nucleotide (NAD) substrate; acute cerebral infarction The present invention relates to an isoquinoline compound represented by the following formula (I) or (II), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction.
WO2008034535A1 Method for treating skin by administering an agent that decreases gmcsf release from keratinocytes Suggested is a method for preventing and/or soothing dry skin or reactive skin against external stresses, characterized in that keratinocytes are contacted with an agent that decreases the GMCSF release from keratinocytes.
CN102077894A Chewing gum for preventing and treating cold diseases The invention relates to chewing gun for preventing and treating cold diseases, which comprises the following components in parts by weight: 1.2-2.5 parts of vitamin C, 20-40 parts of glucose syrup, 70-95 parts of gum base, 5-10 parts of starch, 2-5 parts of wet retention agents, 4-10 parts of flavoring additives, 3-10 parts of antioxidants, 10-15 parts of mulberry leaves, 10-15 parts of honeysuckle flower, 10-15 parts of dyer woad leaves, 10-15 parts of the roots of Chinese thorowax, 5-10 parts of mint and 12-18 parts of Astragalus mongholicus. The chewing gum not only has the advantages of reasonable formula, simple process, low cost, good effect and convenient edibility in the prior art, but also has the effects of dispelling wind and heat from bodies, clearing away lung heat and moistening dryness, clearing livers and improving vision, and has an obvious effect of preventing and treating various kinds of cold after being eaten frequently.
CN101836997B Glycerol/fructose composite and preparation method thereof The present invention relates to a preparing method for glycerol/fructose composite. The preparing method comprises the following steps: (1) the composite in preparation consumption by 1,000 bottles comprises the following components by weight part: 25kg of glycerol, 12.5kg of fructose, 2.25kg of sodium chloride and water for injection added to 250,000ml, then stirring to dissolve the components; (2) adding 0.08% active carbon for needles, stirring, keep boiling gently for 15min, and immediately decarburizing and filtering with a titanium filter rod; (3) further adding the water for injection to the required amount, adjusting the pH value to 3.0 to 6.0 by the 0.1mol/L hydrochloric acid solution, filtering with a phi 0.22mu microporous membrane and a phi 0.45mum microporous membrane, and determining (the content and pH value of) the intermediates; (4) filling and capping after the intermediates are determined to be qualified; and (5) sterilizing at high temperature. The product of the present invention achieves the effect of effectively reducing the intracranial pressure, has long duration and avoids the rebound; meanwhile, the urine volume thereof is obviously lower than the same of patients to whom mannitol is administered, thus reducing the load of the kidney; and the product can further provide the patients with certain energy.
WO2014137234A1 Method for fasting-diet therapy The invention relates to medicine and specifically to gastroenterology, and is concerned with fasting-diet therapy. A saline laxative is administered to the patient and food intake is ceased. Beginning the first day of fasting, 1.5-2 liters of purified water are introduced daily in equal portions, and at the end of the day a cleansing enema is given consisting of 1.5-2 liters of purified water having 10 drops of colloidal silver per 1 liter. A psychotherapeutic conversation is held every day, as well as walks of 30-40 minutes 2-3 times per day and gymnastics according to the Japanese system of Nishi. Beginning the second day of fasting, over the course of 16 days, every day at 7:30 the patient is administered 1/3 of a teaspoon of plant organic sorbent in a glass of water, which, a half-hour later, is followed by drinking a glass of water. At 9:30 and 18:30, anthelmintic plant preparation is administered, and at 9:40 and 18:40, 1 capsule of the plant preparation "Catrel" is administered. 1 teaspoon of colloidal silver is administered at both 10:00 and before bed, it is held in the mouth for 6 minutes and then swallowed, and one drop of same is also administered to each of the eyes and the nose.
WO2014157380A1 Therapeutic agent for wounds or fibrosis Provided is a means whereby wounds or organ fibrosis can be easily treated within a short period of time. A therapeutic agent for wounds or fibrosis, said therapeutic agent comprising a substance capable of specifically inhibiting the expression of FoxO1. Preferably, the inhibitory substance is an antisense nucleic acid, an RNAi-inducing nucleic acid, a ribozyme or an expression vector thereof.
CA2221409C Mch2, an apoptotic cysteine protease, and compositions for making and methods of using the same A substantially pure protein that is a member of the apoptotic Ced-3/Ice cysteine protease gene family, Mch2$g(a), and an inactive isoform of it, Mch2$g(b), are disclosed. Isolated nucleic acid molecules that encode Mch2$g(a) and Mch2$g(b), respectively, are disclosed. Pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with the protein or the nucleic acid molecules are disclosed. Fragments of nucleic acid molecules that encode Mch2$g(a) and Mch2$g(b) having at least 10 nucleotides and oligonucleotide molecule comprising a nucleotide sequence complementary to a nucleotide sequence of at least 10 nucleotides are disclosed. Recombinant expression vectors that comprise the nucleic acid molecule that encode Mch2$g(a) or Mch2$g(b), and host cells that comprise such recombinant vectors are disclosed. Antibodies that bind to an epitope on Mch2$g(a) and/or Mch2$g(b) are disclosed. Methods of identifying inhibitors, activators and substrates of Mch2$g(a) are disclosed. Antisense compounds and methods of using the same are disclosed.
WO2013181251A1 Crizotinib hydrochloride salt in crystalline The present invention provides salts of Crizotinib, solid state forms thereof, and pharmaceutical compositions comprising at least one of the salts or solid state forms. The invention includes crystalline forms of Crizotinib hydrochloride salt.
CN103520150A Medical application of vitamin E and vitamin E derivatives serving as G-CSF (granulocyte colony-stimulating factor) secretion inductive agent and cell mobilization agent The invention relates to an application of vitamin E as shown in a general formula I in the specification with the anti-radiation activity, vitamin E derivatives, vitamin E isomers and possible vitamin E stereisomers as well as a medicine composition containing the compounds in the induction of granulocyte colony-stimulating factor (G-CSF) secretion and/or cell mobilization.
US20120270842 Inhibitors of Diacylglycerol O-Acyltransferase 1 (DGAT-1) and Uses Thereof The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease. Compounds and compositions suitable for use in the disclosed methods are also provided.
US7563782 Optically active stereoisomer of efonidipine analogs; R-configuration of the 4-position on dihydropyridine ring; kidney insufficiency; hypercardia; congestive heart failure; cardiomyopathy; arterial sclerosis; antifibrillatory/antiarrhythmia agents; cardiovascular disorders; antiedemic/antiinflammatory There is provided a T-type calcium channel blocker that is optically active 1,4-dihydropyridine compound, a pharmaceutically acceptable salt thereof or a solvate thereof, of formula (1) wherein R1 and R2 are independently of each other C1-6 alkyl group or R1 and R2 together form —CR5R6—CR7R8, —CR5R6—CR7R8—CR9R10— or —CR5R6—CR7R8—CR9R10—CR11R12—, etc., X1 and X2 are independently of each other O or NR13, Ar is optionally substituted phenyl group, etc., Ra and Rb are independently of each other C1-6alkyl group, —L2—NR16R17, CH2O—L2—NR16R17CN, —L2—N(CH2CH2)2NR16 or NR16R17, etc., Y is C1-20 alkyl group, —L3—NR18R19 and * is absolute configuration of R.
US8735579 Benzamides, production thereof, and use thereof as medicaments Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
US20050100617 Method for improving age-related physiological deficits and increasing longevity A method for mimicking the effects of caloric restriction by administration of a food substrate having carnitine or a carnitine derivative and an antioxidant. The food substrate is capable of modulating gene expression in a way similar to caloric restriction.
US20050260282 Novel hypoglycemic agent, diabetes preventive agent, deep sea water concentrate, and method for producing deep sea water concentrate A hypoglycemic agent includes a concentrate obtained by concentrating deep sea water by heating under reduced pressure. A diabetes preventive agent includes a concentrate obtained by concentrating deep sea water by heating under reduced pressure.
CN1829482B Medicine box for treatment of dependence withdrawal Dosage regimens of buprenorphine to treat withdrawal or abstinence syndrome in a drug dependent or opioid tolerant patient who is pregnant are described. The method includes treating withdrawal or abstinence syndrome of the patient by transdermal administration of an amount of buprenorphine effective to reduce withdrawal symptoms. For example, a first buprenorphine-containing transdermal dosage form for a second dosing period that is no more than about 5 days, the second dosage form comprising the same or a greater dosage of buprenorphine than the first dosage form; and a third buprenorphine-containing transdermal dosage form for a third dosing period that is at least 2 days, the third dosage form comprising the same or a greater dosage of buprenorphine than the second dosage form.
CN1732929A Sulbenicillin sodium for injection and process for preparing its formulation Disclosed is a sulbenicillin sodium for injection and process for preparing its formulation, which comprises the following constituents (by weight ratio): Sulbenicillin : sodium hydrogen carbonate : active carbon : water = 1:0.17-0.35:0.01:3. The prepared sulbenicillin sodium can be prepared into freeze-dried powder, powder injection, or freeze-dried power injection.
US20090246284 O-desmethylvenlafaxine Cocrystals Disclosed herein are co-crystals comprising O-desmethylvenlafaxine and succinic acid, process for the preparation, pharmaceutical compositions, and method of treating thereof.
CN103463013A Preparation process of high-concentration compound amino acid injection The invention provides a preparation process of high-concentration compound amino acid injection. The preparation process of the high-concentration compound amino acid injection is characterized by comprising the following steps of (1) pretreatment by preparation tanks and pipelines; (2) injection preparation process; (3) filling; (4) sterilization; and (5) packaging. The injection preparation process comprises the following steps of grouping and charging according to different amino acid solubilities and solubility characteristics, and dissolving in batches at the water temperature of 70 DEG C according to the difficulty level; closing the preparation tanks after complete dissolution, extracting air in a thick mixing tank and a thin mixing tank respectively until the pressures in the tanks are negative pressures, and introducing high-purity nitrogen into the tanks until the pressures are positive pressures; meanwhile flushing activated carbon in a titanium bar back into the thick mixing tank by water for injection; and then removing carbon for a medicine liquid in the thick mixing tank by the titanium bar, transferring the medicine liquid to the thin mixing tank, and making up to volume by the rest water for injection with prescribed dose to full quantity after the transferring is completed. The problems that the high-concentration compound amino acid injection is yellow in color, the content of tryptophan and the like is lowered excessively, and the amino acid injection is unstable in quality during a storage period are solved.
CN101791317A Compound preparation for treating knee osteoarthritis The invention relates to a compound preparation for treating knee osteoarthritis. Specifically, the compound preparation is formed by brucine or medicinal salts thereof and sodium hyaluronate. The compound preparation has good effect on the treatment of knee osteoarthritis, and complementary collaboration function can be obtained when brucine or medicinal salts thereof and sodium hyaluronate are combined in use.
EP2176223A1 Malonamide derivatives with antithrombotic activity The present invention relates to compounds of the formula (I). The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIla and can in general be applied in conditions in which an undesired activity of factor VIla is present or for the cure or prevention of which an inhibition of factor VIla is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
EP2026654A2 Macrophage migration inhibitory factor antagonists and methods of using same Methods of inhibiting one or more biological activities of Macrophage migration inhibitory factor (MIF) polypeptides are provided using an MIF inhibitory compound. The methods include therapeutic methods for treating cancers and inflammatory diseases.
US20100197590 4-AMINO-7,8-DIHYDROPYRIDO[4,3-d]PYRIMIDIN-5(6H)-ONE DERIVATIVES The invention provides compounds of Formula (Ia) or pharmaceutically acceptable salts thereof, as well as the preparation, compositions and uses thereof, where R1, R2, R3, and m are defined as described above.
CN1879672B Effective components of glabrous sarcandra herb - total polyphenol, its preparation method and application The invention relates to a medicine with effective component of plant nodicorn, which is characterized in that: said effective components can be polyphenol and monomer caffeic acid 3, 4- dihydroxyphenylglycol; the monomer caffeic acid 3, 4- dihydroxyphenylglycol is extracted and purified from nodicorn and other plants; the preparation of polyphenol and the extraction of monomer caffeic acid 3, 4-dihydroxyphenylglycol comprise: refluxing and extracting alcohols in different densities, boiling, extracting butanol, macroreticular resinous adsorbent chromatography and positive and passive silicongel chromatography. The invention can treat cancer, attenuate, and treat general bacteria infection.
US6906040 Method for reducing toxicity of combined chemotherapies Compositions and methods are provided for use in the treatment of cancer.
CN101062019A Lappaconitine hydrobromide transparent patch and the preparing method thereof The invention discloses a hydrobromic acid high babbit nail element transdermal paster, which comprises the following steps: allocating 4. 7-5. 3% hydrobromic acid high babbit nail element, 0-9. 6% transdermal absorption promoting agent and 85-95% pressure-sensitive adhesive acrylic resin; adding the hydrobromic acid high babbit nail element into alcohol; hypersonic-dissolving; adding into pressure-sensitive adhesive and accelerant; supersonic-dissolving; mixing evenly; getting solution; adopting slobbering craft; coating the solution on back lining layer; natural-drying the solution; putting into 80 deg. c bake oven; drying; hardening; cooling; covering on covering layer; getting the product. This product possesses convenient usage and good analgesic effect, which transdermal rate can reach 0. 34mug/cm2 . h.
US20110112200 Solid states of o-desmethylvenlafaxine salts The present invention provides crystalline and amorphous salts of O-desmethylvenlafaxine and processes for preparing said salts of O-desmethylvenlafaxine. The present invention further provides pharmaceutical compositions comprising said salts of O-desmethylvenlafaxine.
US20120088814 Methods of modulating an immune response to a viral infection Disclosed herein are methods for treating respiratory disorders via administration of antisense compounds targeting IL-4Rα. Provided herein, for example, are compositions and methods of modulating immune responses to a viral infection in a subject. Also provided, for example, are compositions and methods for managing, treating, ameliorating, preventing and/or delaying the onset of pulmonary inflammation, airway hyperreactivity and/or loss of lung function, or a symptom thereof in a subject during the course of or resulting from a viral infection. Further provided, for example, are compositions and methods of inducing or augmenting hypo-responsiveness, non-responsiveness or tolerance to a virus in a subject. Also provided, for example, are compositions and methods of enhancing the efficacy of a viral vaccine in a subject. In certain embodiments, the compositions and methods provided herein utilize an antisense compound 12 to 35 nucleobases in length targeted to a nucleic acid molecule encoding human IL-4 receptor alpha IL-4Rα, wherein said antisense compound inhibits expression of human IL-4Rα protein and/or expression of functional IL-4 and IL-13 receptors.
CN101301277A Freeze-dried injection of Meglumine Glycididazole and preparation thereof The invention relates to a freeze-dried powder injection for meglumine glycididazole, which contains the meglumine glycididazole, a pharmaceutical carrier and a pH value regulator. According to the property of the meglumine glycididazole compound, a freeze drying process is adopted to prepare the meglumine glycididazole compound into the freeze-dried powder injection, thereby providing the clinical application with the meglumine glycididazole freeze-dried powder injection with reliable stability, safety, effectiveness, and convenient use. And a method for preparing the meglumine glycididazole freeze-dried powder injection is provided.
US8063045 Fluoropyrrolidines having dipeptidyl peptidase enzyme inhibitory activity The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
CN101284002A Medicine for preventing and curing liver injury The invention relates to a medicine with icaritin as the active component for treating hepatic injuries. The pharmacological experiment shows that the icaritin has antiapoptotic, antioxidant and antiphlogistic activities and protective effects on hepatic injuries; and has evident inhibiting effects on the release of active oxygen, cell apoptosis factor and inflammatory cell factor caused by acute and chronic hepatic injury, anoxic hepatic injury and ischemia-reperfusion hepatic injury. The acute toxicity test of the icaritin on a mouse shows that the icaritin has no toxicity. Therefore, the icaritin has wide development prospect, and can be used for preparing new drugs for preventing and treating the acute and chronic hepatic injury, the anoxic hepatic injury and the ischemia-reperfusion hepatic injury.
WO2008065726A1 Telomelysin-containing agent for breaking antitumor tolerance It is intended to provide an agent for breaking antitumor tolerance. This agent for breaking antitumor tolerance is characterized by containing a recombinant virus carrying a polynucleotide, which has a human telomerase promoter, an E1A gene, an IRES sequence and an E1B gene in this order, having been integrated thereinto.
WO2013131424A1 4-quinazoline amine derivative and application thereof A 4-quinazoline amine derivative as represented by formula (1), a pharmaceutical composition comprising the derivative, and an application thereof in preparing medicine for curing cancer. The cancer is a drug-resistant cancer, preferably a cancer resisting an EGFR reversible inhibitor, and more preferably, a cancer resisting gefitinib, erlotinib or lapatinib; alternatively, the cancer carries EGFR mutation.
US20090062263 4-Hydroxy-5,6-dihydro-1H-pyridin-2-one compounds The invention is directed to 4-hydroxy-5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
US20110082125 Topical Ophthalmic or Otic Solution Formulations Containing Moxifloxacin Hydrocholoride and Dexamethasone Phosphate Topical ophthalmic and otic solution compositions of moxifloxacin and dexamethasone phosphate are disclosed.
WO2013134667A1 Modulating afferent signals to treat medical conditions This document provides methods and materials for modulating afferent nerve signals to treat medical conditions such as CHF, CHF respiration, dyspnea, peripheral vascular disease (e.g., peripheral arterial disease or venous insufficiency), hypertension (e.g., age-associated hypertension, resistant hypertension, or chronic refractory hypertension), COPD, sleep apnea, and chronic forms of lung disease where muscle dysfunction is a part of the disease pathophysiology. For example, methods and materials involved in using electrical and/or chemical techniques to block or reduce afferent nerve signals (e.g., nerve signals of group III and/or IV afferents coming from skeletal muscle and/or the kidneys) are provided.
US7189733 Compositions and methods for inhibiting TGF-β This invention provides compounds that are useful for treating patients having a TGF-β-mediated disease, particularly an ALK5-mediated disease. The compounds are represented by formula I: wherein: a-b is CH2CH2, CH2CH2CH2, CH═CH, CH═N, or N═CH; Z is N or C—F; and G is C1-6 aliphatic or a phenyl, naphthyl, or 5-6 membered heteroaryl ring.
WO2012040634A1 Atropisomers of pi3k-inhibiting compounds The invention provides compounds, compositions and methods to treat certain inflammatory conditions or cancers by administering a compound that inhibits PI3K isoforms, wherein the compounds are optically active atropisomers. It provides optically active stereoisomers of a class of pyrazole-containing compounds, which are useful for these methods, and provides methods to obtain these compounds as well as pharmaceutical compositions containing these compounds.
EP2640698A1 Nampt and rock inhibitors Disclosed are compounds of formula (1c) which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.
CN101757066A American ginseng tabellae iodi gurgitis The invention relates to the field of health care foods, in particular to American ginseng tabellae iodi gurgitis, comprising potassium iodate powder, American ginseng powder, dextrin, mannitol, glucose syrup powder, lyophilized honey powder and magnesium stearate. The American ginseng tabellae iodi gurgitis is characterized by comprising 3.0-4.0 parts of potassium iodate powder, 15-25 parts of dextrin, 25-35 parts of mannitol, 8-10 parts of glucose syrup powder, 1.0-2.0 parts of lyophilized honey powder, 1.5-2.0 parts of American ginseng powder and magnesium stearate accounting for 10 percent of the total weight. In the invention, a little of essence can be added to enable the mouthfeel to be more savoury and mellow, and a little of coloring matter can be added to stimulate the appetite. The invention has the advantages of rich nutrition, fatigue resistance, obvious improvement on immunity of a human body, good health care effect and the like.
US20110081385 Compositions and Methods for Sleep Regulation Compositions and methods for the regulation of sleep and circadian rhythms are provided. The compositions are nutritional supplements containing melatonin and one or more vitamins that enhance the effectiveness of melatonin. Preferred vitamins include folic acid, riboflavin (vitamin B2), cobalamin (vitamin B12) or pyridoxine (vitamin B6). The compositions beneficially and advantageously regulate sleep when administered to an individual and are administered to a human or animal suffering from an irregular sleep or circadian rhythm or are administered in anticipation of the development of such an irregularity.
US20110054009 MicroRNA-Based Methods and Compositions for the Diagnosis, Prognosis and Treatment of Prostate Related Disorders Methods and compositions for the diagnosis, prognosis and/or treatment of prostate associated disorders are disclosed.
US20100323036 Nitric Oxide Therapies A method for delivering nitric oxide therapy to a subject can include administering a composition including a nitric-oxide releasing agent and silica to the subject and releasing a therapeutic amount of nitric oxide from the composition.
US20090233985 Compositions and methods for inhibiting hiv infections by inhibiting lerepo4 and glipr The present invention relates to inhibitor molecules of LEREPO4 or GliPR or respective functional homologues thereof including siRNAs, shRNAs, antisense RNAs, antisense DNA and dominant negative proteinaceous mutants of LEREPO4 or functional homologues thereof. The present invention also relates to pharmaceutical compositions and methods for preventing and/or inhibiting HIV infections by inhibiting the function of LEREPO4 or GliPR or respective functional ho mo logues thereof in vivo. Furthermore, the present invention relates to methods of treating, preventing or diagnosing AIDS and/or HIV infections in an individual. Moreover, the present invention relates to diagnostic methods to determine the susceptibility of HIV strains and isolates for such LEREPO4 or GliPR directed treatment.
US20110086111 Polymeric systems for the delivery of anticancer drugs The present invention relates to compositions for the treatment of cancerous tissues in warm-blooded animals containing one or two anticancer agents attached to polymeric carriers having monomer units derived from one or more of N-(2-carboxypropyl)methacrylamide (2-CPMA), N-(3-carboxypropyl)methacrylamide (3-CPMA), N-(2-aminopropyl)methacrylamide (2-APMA) and/or N-(3-aminopropyl)methacrylamide (3-APMA) are also included. Anticancer agents in compositions can be attached to said polymeric carrier by side-chains which can be susceptible to hydrolysis by lysosomal enzymes intracellularly. Compositions can also include a targeting ligand attached to the polymeric carrier, optionally through a second linker.
CN102302480A Applications of taurine in resisting sleep deprivation stress damage The invention discloses applications of taurine in resisting sleep deprivation stress damage. Tests show that under the sleep deprivation condition, taurine can lower the concentration of blood serum cortisol, improve superoxide dismutase content in livers, and maintain body weight. Taurine is showed to have certain application prospects in coping with high-intensity continuous operations.
US7015231 such as (3Z)-3-[(1-methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one; tyrosine kinase inhibitors; for treatment of tumor growth, restenosis, atherosclerosis, pain and thrombosis The present invention is related to aza-oxindole derivatives, compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
WO2008038417A1 Cardiovascular preparation Disclosed is a novel cardiovascular preparation. The cardiovascular preparation comprises a combination of adenosine 5'-triphosphate or a physiologically acceptable salt thereof and taurine.
CN102584858A Levolactate ulifloxacin crystal and preparation method and application thereof The invention provides a levolactate ulifloxacin crystal. The crystal has the following peaks shown as 2theta in an X-ray powder diffraction pattern in which Cu-Kalpha radiation is used: 5.1+/-0.2 degrees, 10.3+/-0.2 degrees and 25.6+/-0.2 degrees. The invention further provides a preparation method of the crystal, a medicinal composition comtaining the crystal, and pharmaceutical applications of the crystal and the medicinal composition. The crystal provided by the invention has high repeatability, and the preparation method is simple and rapid. As proved by an experiment, the crystal is superior to the conventional crystal of the compound on the aspects of solubility, stability, hydroscopic property and in-vivo treatment effect, can be prepared into multiple dosage forms, and has high clinical application potential.
CN103585571A Disease-resistant auxiliary material for chickens The invention discloses a disease-resistant auxiliary material for chickens. The additive for every 100kg of feed comprises the following active components in unit of weight: 30-50g of wild chrysanthemum flower, 20-40g of Barbat Skullcap, 20-40g of immature bitter orange, 20-40g of Mangnolia officinalis, 10-30g of cassia twig, 10-30g of Rhizoma Zedoariae, 10-30g of trichosanthes kirilowii Maxim, 10-30g of Bighead Atractylodes Rhizome, 10-30g of glabrous greenbrier rhizome, 10-30g of Acalypha australis, 10-30g of rhizoma atractylodis, 10-30g of mung bean, 10-30g of notopterygium root, 10-20g of kudzu root, 5-10g of adamantanamine and 5-10g of sulfadiazine sodium. The additive has the advantages of simple proportioning, favorable preventing and treating effects and low medicine residue, and is convenient to use.
EP1866325A2 Novel crystalline pharmaceutical product There are provided crystalline particles of unsolvated Form 1 polymorph of the compound of formula (I), characterised in that the particles are in the form of substantially triangular plates.
US7229990 E.g., tert-Butyl-5-amino-2-methylthio-4-(3-methoxyphenyl)-quinazoline-6 -carboxamide; used in fertility regulation therapies. A bicyclic heteroaromatic compound according to general formula I, or a pharmaceutically acceptable salt thereof, wherein R1 is (3–8C)cycloalkyl, (2–7C)heterocycloalkyl, (6–14C)aryl or (4–13C)heteroaryl; all optionally substituted with one or more substituents; R2 is (1–4C)alkyl, (2–4C)alkenyl, (2–4C)alkynyl, (6–14C)aryl or (4–13C)heteroaryl; R3 is (1–8C)alkyl, (3–8C)cycloalkyl, (2–7C)heterocycloalkyl, (6–14C)aryl or (4–13C)heteroaryl; Y is CH or N; Z is NH2 or OH; A is S, N(H), N(R), O or a bond and B is N(H), O or a bond; X1—X2 is C═C, C(O)—NH, NH—C(O), C(O)—O, O—C(O), C═N, N═C or S or O. The compounds of the invention can be used in fertility regulation therapies.
US20090075937 Lhrh antagonists for the treatment of lower urinary tract symptoms The present invention provides at least one LHRH antagonist for the treatment or prophylaxis of at least one lower urinary tract symptom in mammals which is to be administered in an intermediate dose, which does not cause chemical (hormonal) castration.
US20120076768 Digestive/laxative compositions Described are digestive/laxative compositions and methods of manufacture and use of same. In a preferred embodiment, the invention provides for a digestive/laxative composition including actinidin. The actinidin is preferably contributed by inclusion of fruit of genus actinidia, or a product thereof. Preferably, the process for forming the composition includes a method in which the fruit is processed at a temperature below that causing significant degradation of actinidin present, this temperature being preferably in the range of −40° C. to 40° C. Methods of administration of the composition are also described.
US20080312306 Polymorphs, solvates, and hydrate of 5-(4'-fluoro-2'-oxo-1',2'-dihydrospiro[cyclopropane-1,3'-indol]-5'-yl)-1-methyl-1h-pyrrole-2-carbonitrile Novel polymorph Form II and III, solvate Forms I, II, III, and IV, and the hydrate of 5-(4′-fluoro-2′-oxo-1′,2′-dihydrospiro[cyclopropane-1,3′-indol]-5′-yl)-1-methyl-1H-pyrrole-2-carbonitrile are provided, as are methods for preparing the same. Pharmaceutical compositions and kits containing these novel polymorphs, solvates, and hydrate, and combinations thereof are further provided, as are methods of contraception; treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, hormone-dependent carcinomas; treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; or treating symptoms of premenstrual syndrome using one or more of these polymorphs, solvates, or hydrate.
US20110301115 Methods of Treating Subclinical Sun Damage Provided are methods of treating subclinical sun damage and of inducing a chemocytotoxic response in skin. Methods of treating subclinical sun damage include the steps of: topically administering to skin of a patient a composition comprising a chemocytotoxic agent in an amount effective to induce erythema, scaling, crusting, or combinations thereof and resolve at least a portion of the subclinical sun damage, where the skin has a condition of no clinical sign of sun damage and the patient was not previously treated for actinic keratosis or nonmelanoma skin cancer. The chemocytotoxic agent can comprise a fluorinated pyrimidine antimetabolite such as 5-fluorouracil (FU), 5-fluorouridine (FUR), 5-fluorouridine-5′-monophosphate (FUMP), 5-fluorodeoxyuridine (FUdR), 5-fluorodeoxyuridine-5′-monophosphate (FdUMP), or combinations thereof.
CN101564378A Levocarnitine oral solution and preparation method thereof The invention relates to a levocarnitine oral solution and a preparation method thereof, which belong to the technical field of medicaments. The main drug is levocarnitine, and the pharmaceutic adjuvant comprises a pH regulator, a sweetening agent, mucilage, a flavoring agent and a preserving agent. Each 1,000 milliliters of the prepared oral solution contains 50 to 300 grams of the main drug levocarnitine. The levocarnitine oral solution can be absorbed quickly and has quick action and good curative effect; and by adopting single dose package, the levocarnitine oral solution is convenient to take and carry, has accurate minute dose, small dosage and good taste, and is easy to be accepted by patients. The levocarnitine raw material has stronger hygroscopicity, and has high requirements on the environment (particularly the relative humidity) and rigorous production conditions and is difficult to store if the levocarnitine raw material is prepared into solid preparations; however, the disadvantages can be overcome if the levocarnitine raw material is prepared into liquid preparations.
US6844008 Tablet composition A tablet composition containing N-(trans-4-isopropylcyclohexanecarbonyl)-D-phenylalanine and a disintegrant, selected from a low substituted hydroxypropylcellulose, sodium carboxymethyl cellulose, calcium carboxymethyl cellulose and sodium croscaramellose sodium, is disclosed. This tablet composition is rapidly disintegrated in the stomach after the administration and absorbed without being influenced by meals to inhibit the rise of the blood sugar levels of diabetics after meals.
CN101805337B Compound containing proline and isoxazole skeleton and preparation method and application thereof The invention relates to the medicine filed related to diabetes, in particular to a peroxisome proliferator-activated receptor (PPAR) agonist which has the general formula I shown in the specification, has treatment effect on diabetes and contains proline and an isoxazole skeleton, a preparation method of the PPAR agonist and application of the PPAR agonist in treating diabetes, wherein, the group definition refers to the specification.
CA2261988C Mannose-6-phosphate composition and its use in treating fibrotic disorders Mannose-6-phosphate is formultated by pH adjustment as a suspension or solution at pH 6 to 8, preferably 6.5 to 7.5 and preferably at a concentration of 65 to 300 mM. Suspensions can be made in viscous hyaluronic acid gels. These compositions are useful in wound healing, particularly to prevent or mitigate scar formation.
US20090069257 Method of achieving persistent Transgene expression Non-inflammatory vector compositions are provided that are suitable for repeated transgene delivery and that result in persistent transgene expression. The compositions are non-inflammatory, the present compositions are suitable for readministration and do not induce expression-limiting immune or inflammatory responses. Thus, these compositions are useful in methods of repeated administration to achieve persistent transgene expression, and are especially suited to treating genetic, acquired and inflammation-associated conditions.
CN1879830A An effervescence tablet with stemona root and hairy vein agrimony for treating gynecological inflammation and method for preparing same The invention discloses effervescent tablets for treating gynaecologic inflammation and its preparation comprising the following steps: grilling flavescent sophora root, roor of sessile stemona, cnidium fruit, hairy vein agrimony and purple perilla, merging the grilling liquid, filtering and concentrating the filtrate into thick grease with specific gravity of 1.05-1.15 (60 deg C), stewing 24-4 hours, filtrating, reclaiming ethanol from the filtrate, concentrating to obtain clear grease, drying, disintegrating and passing through 80 mesh sieve, disintegrating other herbs and auxiliary materials, passing through 80 mesh sieves. The raw materials also include ammonia alum, sodium hydrogen carbonate, lactose, boracic acid, citric acid, hydroxypropyl cellulose, boneol, camphor and dodecyl sodium sulfate.
US20050070500 Method of modulating release of saccharides and uses thereof The present invention relates to a method of controlled release of saccharides and oligosaccharides in human and animal. Polysaccharides are digested in a manner to provide oligomers having desired numbers of units of saccharides or monosaccharides, most particularly glucosamine and N-acetyl-glucosamine and derivatives thereof. The rate of release of monosaccharides is proportional to the length of the oligomers administered to an organism, and has targeted physiological effects depending on the length of the oligomers used.
CN102552233A Application of methyl 3, 4-dihydroxybenzoate in preparation of medicaments for preventing and treating nerve degenerative diseases The invention discloses the application of methyl 3, 4-dihydroxybenzoate (MDB) in preparation of medicaments for preventing and treating nerve degenerative diseases. According to the invention, MDB or derivatives thereof have double functions of maintaining survival of neurons or nerve cells and promoting growth of nervous processes, can be applied to develop neurotrophic factor mimetic agents for treating nerve degenerative diseases (such as AD and PD) and other related diseases, and can also be applied to cell and gene transplantation therapy for nerve degenerative diseases (such as AD and PD) and other related diseases. The invention determines new pharmacological activity of MDB and illuminates pharmacodynamic mechanism of MDB, and provides reference for developing new drugs with independent intellectual property rights.
CA2403871C Inhibition of angiogenesis and tumor growth Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.
CN101601643A Skeleton hemostasis gel The invention provides a skeleton hemostasis gel and is characterized in that the gel is composed of 1-99 parts by weight of sulfhydrylated multi-branched polyethylene oxide, 99-1 parts by weight of sulfhydrylated chitosan and 0-90 parts by weight of cross linking agent. The invention has the advantages that hemostasis effect is good, the gel can be completely absorbed and degraded, histology of medullary cavity of skeleton after complete absorption is in normal condition, and the gel has certain osteogenesis simulation function without influencing fracture healing or stability between the skeleton and prosthesis, promotes bone formation and improves bone ingrowth between the skeleton and the prosthesis.
US20100280034 Modulation of pathogenicity The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C═O, C═S, SO2, CH—OR13, C═NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C═O, C═S, SO2, CH—OR13, C═NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;
US8097274 Skin substitutes, preparation methods and uses thereof Provided herein are skin substitutes suitable for use in a living subject for purpose of repairing damaged tissues, methods of producing the skin substitutes and their uses. A biocomposite membrane comprising poly(ε-caprolactone) (PCL) and at least one material selected from collagen and gelatin is provided. In one embodiment, the biocomposite is a 2-component membrane of PCL and gelatin. In another embodiment, the biocomposite is a 3-component membrane of PCL, collagen and gelatin. The bio-composite membrane may be used directly in vivo as a wound dressing, or as a support for cell growth on each side of the membrane to produce an in vitro cultivated artificial skin for future in vivo and/or in vitro applications.
CN103191065A Celecoxib new formulation and preparation method thereof The invention discloses a celecoxib pellet preparation, which is used for treating rheumatic arthritis, osteoarthritis and ankylosing spondylitis, and also can be used for treating acute pain, dysmenorrheal, colorectal polyps, post-operation analgesia, low back pain, periarthritis of shoulder and tenosynovitis. According to the celecoxib new formulation and the preparation method thereof, the pellet preparation technology and the controlled-release pellet upper covering technology are adopted and microcrystalline cellulose pills are selected for dissolving the celecoxib material medicines in adhesive povidone solution, the medicine materials are uniformly sprayed on the surface of the pills and covered with isolating layers, so that the pellet is pressed and capsule. When the disintegration time limit of the celecoxib pellet preparation is remarkably shortened and the bioavailability is remarkably improved.
US20080247996 Methods of treating neoplasia with combination target cell-specific adenovirus, chemotherapy and radiation The invention provides methods of treating neoplasia using combinations of target cell-specific replication competent adenoviral vectors and chemotherapy, radiation therapy or combinations thereof. The adenoviral vectors are target cell-specific for the particular type of neoplasia for which treatment is necessary and the combination with the chemotherapy and/or radiation leads to synergistic treatment over existing adenoviral therapy or traditional chemotherapy and radiation therapy.
CN101380329B Preparation method of arginine aspirin and powder and injection preparation thereof The invention discloses an aspirin arginine and a preparation method of powder for injection thereof, the preparation method is characterized in that: arginine is dissolved in water, aspirin is further added, the arginine fully reacts with the aspirin in the water by stirring at the reaction temperature of 60-80 DEG C, chloroform is added after the reaction, the low temperature preservation, the precipitation and the filtration are carried out, sediment is washed and vacuum dried, an aspirin arginine crude product is obtained, and then the aseptic packaging or the freeze-drying after the redissolution is carried out to obtain the aspirin arginine powder for injection. The method has short reaction time and high production efficiency, and the obtained aspirin arginine powder for injection has stable product quality.
US20050222100 Treatment of post-menopausal complaints in breast cancer patients comprising tibolone and a serm The subject invention provides a use of tibolone and a SERM for the manufacture of a medicine for the treatment of an estrogen-deficiency related complaint and for the prevention of a recurrence of breast cancer in females suffering from, or at risk for breast cancer that exhibit the estrogen-deficiency related complaint.
CN102070631A Quaternary ammonium salt of penehyclidine optical isomer, medicinal composition and medical application thereof The invention relates to a quaternary ammonium salt compound shown as a formula I, or pharmaceutically acceptable salt or solvate thereof. The invention also relates to application of the compound as a selective M receptor antagonist, particularly a selective M3 receptor antagonist, and a compound-containing medicinal composition.
CN103610645A Pharmaceutical composition with fexofenadine hydrochloride and preparation method of pharmaceutical composition The invention relates to a pharmaceutical composition with fexofenadine hydrochloride. The composition is composed of the following components: 1-12% of fexofenadine hydrochloride as an active ingredient, 1-10% of suspending aid, 5-85% of filler, 1-10% of sweetening agent, 0.01-10% of essence and a conventional amount of flow aid, wherein the composition exists in a form of a dry suspension. The fexofenadine hydrochloride suspension provided by the invention has the advantages of high dispersity, uniformity in distribution, rapidness in absorption, high bioavailability, good taste, stability and the like.
CN101032523A Royal jelly acid calcium and preparation process thereof The present invention is royal jelly acid-calcium and its preparation. Royal jelly acid-calcium is prepared with the materials including calcium lactate, freeze dried royal jelly powder, freeze dried sour milk powder, mannitol, glucose, dextrin and magnesium stearate, and through mixing. Royal jelly acid-calcium can raise body's immunity, delay senility, antagonize invasion of high temperature, cold, anoxia, fatigue and rays, provide body with vitamins, amino acids and mineral matters, favor the absorption and utilization of calcium, etc.
CN1857279A Hysteromyoma treating suppository and its preparing method The present invention discloses a kind of hysteromyoma treating suppository and its preparation process. The hysteromyoma treating suppository is prepared with danozol 10-20 wt%, stearic acid 10-20 wt% and semi-synthetic fatty acid ester 60-80 wt%. The preparation process includes the following steps: heating stearic acid and semi-synthetic fatty acid ester in water bath at 60-90 deg.c; adding danozol after cooling to 40-50 deg.c; preparing in hot smelting process and sealing and packing. The present invention has the beneficial effects of: raised curative effect, reduced toxic side effect on liver of the medicine, less stimulation on stomach, etc.
CN102993174A Dabigatran etexilate derivative as a prodrug The invention relates to a preparation method of a benzimidazole derivative represented by the general formula I, wherein R1 and R2 are respectively defined in the specifications. The invention relates to a dabigatran etexilate derivative represented by the general formula I, a non-toxic pharmaceutically acceptable salt thereof, medicine compositions comprising the compounds as active components, and applications of the compounds and the medicine compositions as thrombin inhibitors. The general formula I is represented below.
EP1097141B1 Imidazole derivatives with biphenylsulfonyl substitution, method for preparing them and their use as a drug or diagnostic agent The invention relates to compounds of formula (I), wherein the symbols have the meanings indicated in the specification. The inventive compounds exhibit dramatic antiarrhythmic proprieties and contain a cardioprotective compound. They can preventively inhibit or strongly reduce pathophysiologic processes upon occurrence of ischemic injuries, especially ischemic cardiac arrhythmia. Said compounds also exhibit a strong inhibiting effect on cellular proliferation.
WO2012065958A9 Method of treating contrast-induced nephropathy The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula (I) wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.
CN103656343A Medicine for treating gastric ulcer, and preparation method of medicine The invention discloses a medicine for treating gastric ulcer, and a preparation method of the medicine. The medicine is mainly prepared by cuttlebone, semen euryale, semen coicis, concha arcae, rhizoma corydalis, radix polygonati officinalis, fructus perillae, stalactite, liquorice, rhizoma cyperi and the like according to a certain weight proportion. The medicine has functions of regulating a middle warmer, relieving contracture, resolving phlegm, moistening a lung, and coordinating drug actions, has a fast effect on treating the gastric ulcer, and is short in treatment course, and the gastric ulcer does not relapse after cured.
CN101810626B Contraceptive medicament preparation containing gestodene The invention relates to a contraceptive medicament preparation containing gestodene, which is dosed through natural orifice of human beings or mammals or through transdermal or subcutaneous administration. The gestodene is in a zero order release pattern. The contraceptive medicament preparation contains 0.0005 mg to 0.100 mg of gestodene of daily dose, and one or more kinds of pharmaceutical acceptable excipient or carriers. The contraceptive medicament preparation is characterized in that the gestodene is a crystal or powders with the weight specific surface area more than 100 cm2/g. The minimal distance between the geometric center of the crystal with more than or equal to 70% of weight proportion and the surface of the preparation is less than or equal to 5 mm. The minimal distance between the geometric center of the powders with more than or equal to 70% of weight proportion and the surface of the preparation is less than or equal to 5 mm. The contraceptive medicinal preparationcontains 0.005 mg to 0.050 mg ethinyloestradiol of daily dose. In the invention, the distribution characteristics of the size and the design of the drug is selected, the drug can be in a better zero order release pattern, and the cumulative release rate is higher.
WO2012036180A1 Xanthone derivative and use thereof Provided is a novel compound having excellent anticancer activity and metastasis inhibition activity. An α-mangosteen diester represented by general formula (1): (in the formula, R1 represents the residue after a hydroxyl group is removed from a C8-14 medium chain triglyceride), and an anticancer agent or metastasis inhibiting agent including said compound as the active component thereof.
US20130029987 Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
WO2008067709A1 Substituted cyclobutane compounds, preparation methods and pharmaceutical uses thereof Substituted cyclobutane compounds represented by formula I or II. The preparation method of these compounds and uses thereof as glucagons like peptide-1 receptor(GLP-1R) regulators for preventing and/or treatment of metabolic disorders, which include but not limit to diabetes, insulin-resistance and obesity etc., cardiovascular diseases and neurodegenerative diseases such as Alzheimer's diseases etc..
WO2013057287A1 Pharmaceutical compositions comprising dgla and/or 15-hetre and methods of use thereof The present disclosure provides compositions comprising fatty acids, or derivatives thereof (e.g., C1-C4 esters) including, for example, DGLA, and/or 15-HETrE, used singly or in combination for the prevention and/or treatment of effects associated with UV radiation such as erythema.
CN101756911A Novel sodium ozagrel preparation and preparation method thereof The invention relates to a novel sodium ozagrel preparation and a preparation method thereof. The method mainly includes the following steps: (1) adding prescribed amount of sodium ozagrel material and sodium hydroxide into appropriate amount of water for injection to be fully dissolved; (2) ultra-filtering to remove the pyrogen; (3) adjusting the pH; (4) degerming, filtering and filling; (5) freeze-drying and capping. By adopting ultra-filtration method to remove the pyrogen, the method has the advantages of high pyrogen removal efficiency, strong selectivity and less insoluble particles as compared with the conventional pyrogen removal method through active carbon, so the safety of the product is greatly improved and the quality is more reliable.
WO2010106460A1 A dermaceutical cream made using sodium fusidate, miconazole nitrate and fluticasone propionate The invention discloses a dermaceutical cream containing Fluticasone Propionate as a steroid, Miconazole Nitrate as an antifungal agent and an antibacterial agent in the form of Fusidic acid, which Fusidic acid is formed in situ from Sodium Fusidate as the starting raw material, wherein Sodium Fusidate is converted into Fusidic acid under oxygen-free environment. The cream of the present invention has greater shelf- life stability and the finer particle size of the API than the conventional creams containing Fusidic acid. The cream of the present invention has greater shelf-life stability and the finer particle size of the API than the conventional creams containing Fusidic acid. The cream of the present invention contains Fusidic acid as the API that has been formed in situ from Sodium Fusidate, Miconazole Nitrate as an antifungal and Fluticasone Propionate as a steroid, in a cream base comprising a preservative, an acid, a co-solvent, emulsifiers and a waxy material along with water, preferably purified water.
CN102743329A Novel intrauterine sustained control release drug delivery system and preparation method thereof The present invention relates to a female intrauterine drug delivery system, and more particularly to a novel intrauterine sustained control release drug delivery system and a preparation method thereof. The present invention provides a novel intrauterine sustained control release drug delivery system and a preparation method thereof, wherein the system has characteristics of short length, light weight, efficiency, and reversibility. The system comprises a sustained control release pipe, a drug core and a tail filament, wherein the sustained control release pipe is wrapped on the external of the drug core, the tail filament is positioned between the sustained control release pipe and the drug core or is accomodated in the middle of the drug core, the drug core is a rod prepared by blending progesterone or an available intrauterine sustained control release drug and a biodegradable polymer, and the sustained control release pipe is made of a silicon rubber. The system of the present invention has characteristics of no stent, no copper ion, safety, practicality, and simple placement technology.
US20080021013 JAK inhibitors for treatment of myeloproliferative disorders The invention provides a method for treating myeloproliferative disorders, myelodysplastic syndromes and other diseases, in which activation of JAK2 contributes to pathology, in a mammal comprising administering to the mammal an effective amount of a fused pyrrolocarbazole derivative wherein the fused pyrrolocarbazole derivative inhibits the activity of JAK2.
US8518999 Modulators of TNF-αsignaling The present invention provides compounds which are modulators of TNF-α signaling and methods of use thereof for treating a patient having a TNF-α mediated condition. The compounds can be represented by the following structural formulas:
US20120225021 Stable colloidal gold nanoparticles with controllable surface modification and functionalization In the present invention, a method of producing stable bare colloidal gold nanoparticles is disclosed. The nanoparticles can subsequently be subjected to partial or full surface modification. The method comprises preparation of colloidal gold nanoparticles in a liquid by employing a top-down nanofabrication method using bulk gold as a source material. The surface modification of these nanoparticles is carried out by adding one or multiple types of ligands each containing functional groups which exhibit affinity for gold nanoparticle surfaces to produce the conjugates. Because of the high efficiency and excellent stability of the nanoparticles produced by this method, the fabricated gold nanoparticle conjugates can have surface coverage with functional ligands which can be tuned to be any percent value between 0 and 100%.
US6887891 Derivatives of lipoic acid, their preparation, their use as medicaments and the pharmaceutical compositions containing them Compounds of formula wherein the substituents are as defined in the specification which compounds are useful for inhibiting the activity of NO-synthase enzymes.
US20100021468 Novel mhc class ii restricted t cell epitopes from the cancer anitgen, ny eso-1 The present invention discloses the identification and isolation of novel MHC class II epitopes derived from the cancer antigen, NY ESO-1. The novel MHC class II epitopes from NY-EsO-1 are recognized by CD4+ T lymphocytes in an HLA class II restricted manner, in particular HLA-DR or HLA-DP restricted. The products of the gene are promising candidates for immunotherapeutic strategies for the prevention, treatment and diagnosis of patients with cancer.
CN102100698A New clinical use of pharmaceutical composition The invention relates to a new clinical use of a pharmaceutical composition, which is characterized in that the composition formed by citicoline salt and inosine or adenosine can be applied in the preparation of a medicament for treating cerebral vascular functional disorder, craniocerebral injuries, dementia, Parkinson disease and heart diseases. The use amount of the citicoline salt per unit is 0.01g-2.5g; and the use amount of the inosine per unit is 0.005g-2g.
CN101003811A Citron gene of human, coding protein, and application This invention discloses human Citron gene and its coded protein. This invention also discloses the application of human Citron gene in anti-tumor drugs. By inhibiting the expression level through RNA interference, the human Citron gene can inhibit the growth of hepatocarcinoma cell, thus can be used as a new treatment target for developing anti-tumor drugs.
CN102988341A Tissue specificity proteasome inhibitor and application thereof The invention discloses a tissue specificity proteasome inhibitor, and application of the tissue specificity proteasome inhibitor in preparation of a medicament for inhibiting tumor proteasome. The tissue specificity proteasome inhibitor is gambogic acid and/or a metabolite MT1 of the tissue specificity proteasome inhibitor.
WO2013142912A1 Methods and compositions for reducing ocular discomfort The invention relates to compositions and devices which include an osmolytic agent, in particular a betaine or carnitine compound, for reducing ocular discomfort associated with various diseases or conditions, in particular diseases or conditions associated with high tear film tonicity. The invention also relates to methods of treating or preventing various diseases or conditions using compositions and devices of the invention.
EP2658560A1 A nutritional composition comprising fiber and probiotics for reducing stress-related intestinal symptoms The present invention provides a nutritional composition that is suitable to reduce the impact of stress on intestinal symptoms and/or conditions. The composition comprises one or more selected from a probiotic microorganism,one or more inactive probiotic, and one or more culture medium of one or more probiotic; and soluble fiber, and possibly other ingredients such as a milk ingredient, a source of carbohydrates and a source of protein. Preferably, the soluble fiber is a low viscosity soluble fiber. The composition is in particular suitable to alleviate abdominal discomfort, abdominal pain, abdominal cramps, and bowel movement disturbances, such as abdominal bloating, flatulence, in particular in as far as these conditions and symptoms are associated with stress.
EP0789567B1 A method for treating vascular headaches The present invention provides methods for treating migraine headache. The methods useful according to the invention involve the treatment of patients who experience symptoms of migraine headache with compounds that directly or indirectly activate GABAA receptors.
EP2490680A2 Neuroprotection and myelin repair using nestorone® Methods for treating neurodegeneration and/or myelination in patients are disclosed comprising treating the patient with a progestin compound which exerts binding to progesterone receptors and elicits progesterone-receptor-induced biological responses without interacting with the androgen receptor and without inducing androgen or glucocorticoid biological responses at a dosage sufficient to prevent or reduce neurodegeneration. The progestin compound preferably comprises 16-methylene-17α-acetoxy-19-norpregn-4-ene-3, 20-dione, and the methods include combining the progestin compound with an estrogen compound to provide both contraception and treatment for myelin repair and neurodegeneration.
EP1968609A2 Pharmaceutical compositions and methods of use of highly lipophilic sulfhydryl compounds Novel compositions of silicon-containing sulfhydryl compounds, their preparation and use in methods for treating disease are described. Silicon confers lipophilicity that can enhance the penetration of the silicon derivative sulfhydryl compounds across the gut wall, cell membranes and blood brain barrier, thus improving therapeutic properties including bioavailability, metabolism, and/or pharmacokinetics. The organosilyl group provides compounds having improved pharmacokinetics. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
CN101926761A Production method of compound potassium dihydrogn phosphate The invention relates to a production method of compound potassium dihydrogn phosphate injection, which comprises the following steps in turn: material preparation, decoloration, encapsulation, sterilization, leakage detection, lamp inspection, bottle boiling, lettering and packaging. The production method also comprises heating-cooling treatment for at least one time after the encapsulation stepand before the packaging step, and the heating-cooling treatment is to heat the injection to 40 to 100 DEG C first and then allows the injection to cool naturally to room temperature. No crystals precipitate from the injection provided by the invention even in a shock cooling environment or in a low-temperature storage environment, so that the quality and the use performance of the product are guaranteed.
US20110064687 Mono-, di- and polyol phosphate esters in personal care formulations A hydrophilized personal care formulation, which can be in the form of a hand or body soap (liquid or bar), lipstick, body wash, makeup remover, skin cleaner, hair conditioner, skin or hair moisturizer. The formulation employs an organophosphorus material or a mixture of an organophosphorus material, for example, mono-, di-, and polyol phosphate esters.
US20070292507 Supportive Treatment of Liver Disease The invention provides a composition and method for treatment of a subject suffering from liver disease comprising the oral administration of a slow release formulation of calcium channel blocker such as diltiazem and thiamine which is also an antioxidant which is relatively hydrophilic when compared with the calcium channel blocker.
US20100034873 Transdermal ricinoleic acid compositions Transdermal compositions containing castor oil are described. The compositions comprise ricinoleic acid and a transdermal vehicle with optional additional agents. One optional additional agent is an adrenergic drug which may cause the ricinoleic acid to penetrate the skin more deeply and have a longer lasting effect. The compositions can be used for treating a variety of ailments traditionally treated with castor oil or castor oil packs, without the mess and inconvenience of using castor oil packs.
CN101057827A Palonosetron injection and its preparation method The invention discloses a palonosetron injection and the preparation method. The essential component of the injection comprises: hydrochloric acid palonosetron 0. 01-0. 05 mg/ ml, glucose 45-55 mg/ ml, aminoacetic acid 0. 2-10 mg/ ml. The preparation method comprises following steps: (1) dissolving hydrochloric acid, glucose, and aminoacetic acid in proper amount of water for injection, moderating pH value, adding water for injection to meet the demand; (2) filtering with micro-porous membrane; (3) packing filtered solution, aerating inert gas or carbon dioxide, pressing, covering. The product is characterized by low production cost and good stability.
CA2192089C Inhibitors of interleukin-1.beta. converting enzyme The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
CN101795690A Method for reducing intracranial pressure The present invention relates generally to methods for reducing intracranial pressure in a subject. More particularly, the methods of the present invention include administering to the subject an effective amount of a substance P receptor antagonist.
WO2006037348A1 Pharmaceutical compositions comprising fenofibrate and a statin Pharmaceutical compositions in particulate form or in solid dosage forms comprising a combination of a reduced or low dose of fenofibrate and an HMG CoA reductase inhibitor selected from the group consisting of lovastatin, pravastatin, rosuvastatin, pitavastatin and fluvastatin or a pharmaceutically active salt thereof. The statin is optionally provided as a controlled release or a delayed release formulation, which may result in a maintained LDL-lowering effect at a reduced dosage. Fenofibrate is provided in a formulation being bioequivalent to commercially available Antara® capsules, or exhibiting increased bioavailability as compared therero, and also reduced food effect.
US6964959 Use of a methylol-containing compound to treat tumors The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing methylol-containing compound. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis.
WO2008076779A3 2-(piperidin-4-yl0xy)pyrimidin-4-amine derivatives as deoxycytidine kinase inhibitors for the treatment of cancer A deoxycytidine kinase inhibitor of formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein: L1 is a bond (i.e., the nitrogen is directly bound to A), -C(O)-, -SO2-, or -C(R4)2-; A is optionally substituted alkyl, aryl or heterocycle; R1 is hydrogen, halogen, -OH, -NH2, -NO2, -CN, -C(O)OR4, or optionally substituted alkyl; R2 is hydrogen, halogen, -OH, -NH2, -NO2, -CN, -C(O)OR4, or optionally substituted alkyl; each R3 is independently =O or optionally substituted lower alkyl; each R4 is independently hydrogen or lower alkyl; n is 1-3; and m is 0-3 if n is 1, m is 0-4 if n is 2, or m is 0-5 if n is 3, for the treatment of cancer.
CN1911933A Oxygen, nitrogen heterocyclic naphthoyl imine kind compound and its bioapplication The present invention relates to one kind of naphthyl imide compounds with oxygen heterocycle and/or oxygen heterocycle and its use. The naphthyl imide derivatives of the present invention have the structure as shown. The naphthyl imide derivatives the present invention designs and synthesizes have the effect of inhibiting the growth of tumor cells of different tissue sources and genetic varied cells of different sources.
US20130245575 Body product and method of delivery A composition and method for administering topical and external topical and external body products for prevention and treatment of anal/vaginal ailments, the composition comprising a mixture of a melting agent, a healing agent, a hardening agent a moisture barrier agent, a carrier agent, the mixture in solid state and undergoing a phase change to a lubricating state when applied to a human body.
US7393944 Lymphocytes; transcription factors; interferons Isolated nucleic acid molecules encoding T-bet, and isolated T-bet proteins, are provided. The invention further provides antisense nucleic acid molecules, recombinant expression vectors containing a nucleic acid molecule of the invention, host cells into which the expression vectors have been introduced and non-human transgenic animals carrying a T-bet transgene. The invention further provides T-bet fusion proteins and anti-T-bet antibodies. Methods of using the T-bet compositions of the invention are also disclosed, including methods for detecting T-bet activity in a biological sample, methods of modulating T-bet activity in a cell, and methods for identifying agents that modulate the activity of T-bet.
CN101965352A Pyripyropene derivative having acat2-inhibiting activity Disclosed are: a compound represented by the general formula (I), (II) or (III), or a pharmacologically acceptable salt, solvate or hydrate thereof,and a pharmaceutical composition comprising the compound or the pharmacologically acceptable salt, solvate or hydrate thereof as an active ingredient. The compound has an excellent ACAT2-inhibiting activity, and the mechanism of action of the compound is different from that of a statin-containing pharmaceutical agent. Therefore, the compound can be used as a therapeutic or prophylactic agent for obesity,adiposis,hyperlipemia,hypercholesterolemia,metabolic dyslipidemia,arteriosclerosis,hyperlipemia, hypercholesterolemia, metabolic dyslipidemia, arteriosclerosis or hypertension induced by obesity,or the like.
US20130190400 Method for producing gamma-aminobutyric acid and food produced thereby The embodiment of invention provides a method for producing γ-aminobutyric acid, including the steps of providing a medium including Saccharomyces cerevisiae, adding an extract of Rhinacanthus nasutus into the medium and fermentating Saccharomyces cerevisiae in the medium added with the extract of Rhinacanthus nasutus to produce γ-aminobutyric acid.
US20120232025 Safener drug combinations for use with nmda antagonist drugs Prolonged administration of subanesthetic dosages of ketamine, which suppresses activity at NMDA receptors, can provide a damaged central nervous system with an opportunity to use its innate healing processes to “reset” NMDA receptors which were pushed into an unwanted hyper-sensitized state by unusually high activity. However, such treatments can cause permanent brain damage, if the ketamine dosage is too heavy or prolonged. Certain types of “safener” drugs have previously been identified, which can block or at least reduce those unwanted side effects. It is disclosed that if two classes of safener drugs are combined, which will simultaneously suppress activity at both (i) muscarinic acetylcholine receptors, and (ii) the kainate and AMPA classes of glutamate receptors, those safener drug combinations can provide exceptionally potent and reliable safening activity, which can enable the safe use of potent NMDA antagonist drugs for a number of highly beneficial purposes.
US7265110 Psychological disorders; antidepressants; anxiolytic agents; analgesics; antiinflammatory agents; central nervous system disorders The present invention relates compounds of the formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, and R10 represent a variety of substituents; A represents NR9 or O; B represents a bond, CH2, NR9 or O, wherein one or both hydrogen atoms in said CH2 moiety may be replaced with one or both of R7 and R8, or alternatively, one of the hydrogen atoms in said CH2 moiety together with a hydrogen atom from an adjacent carbon are replaced by a double bond; with the proviso that when A is O, then B is NR9; n is zero, 1 or 2; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia
CN103121998A Vinpocetine compound and drug composition thereof The invention belongs to the technical field of medicine, and particularly relates to vinpocetine compound. The vinpocetine compound is shown in an X-ray powder diffraction spectra I measured by a Cu-K alpha ray. A preparation method of the vinpocetine compound, and a drug composition containing the vinpocetine compound are also provided by the invention. The vinpocetine compound disclosed by the invention is long in storage time, less in impurity content, and good in storage stability; and the drug composition containing the vinpocetine compound is good in storage stability and high in safety performance.
US20080020997 Glucosamine and Glucosamine/Anti-Inflammatory Mutual Prodrugs, Compositions, and Methods Mutual prodrugs of glucosamine, and derivatives and analogs of glucosamine and an anti-inflammatory agent, compositions thereof, and methods for, e.g., treating disorders and conditions by administration of the compositions are provided. Topical compositions of glucosamine, and derivatives and analogs of glucosamine are also provided.
CA2726883A1 New terpenes and macrocycles Novel terpenes and macrocycles are activators of TGR5 and can be used for the prevention and/or treatment of Diabetes Typ 2, obesity, neuropathy and/or nephropathy.
EP1218366B8 Method for producing cox-2 inhibitors The invention relates to a method for producing compounds of general formula (I) wherein R1 is selected from the following groups: (a) OR5 and (b) mono-, di-, or tri-substituted phenyl; and R2 represents a group (C1-C6)alkyl. The method is characterised in that it comprises the following steps: a) reacting a compound of general formula (II) with an acid of general formula R1CH2 COOH (III) in a water-free medium; b) reacting the resulting compound with a strong base in an aprotic solvent in order to obtain an intermediate cyclic compound which forms a compound of general formula (I) after dehydration; and c) isolating said resulting compound of general formula (I).
WO2008119260A1 A medicinal composition of carmustine, preparation method and application The invention discloses a medicinal composition of carmustine, comprising cure effective quantity of carmustine, Tween type surface active agent and latent solvent. The latent solvent is chosen from one or more of glycerin or polyethyleneglycol. This composition can be injection or frozen powder injection. Solubility of carmustine can be increased by adding Tween and latent solvent. This invention further discloses method of preparing this medicinal composition.
US20120252856 Pi3k/akt pathway subgroups in cancer: methods of using biomarkers for diagnosis and therapy The present invention relates to methods of dividing cancer into subgroups based upon Akt pathway gene expression. In one embodiment, the present invention provides a method of diagnosing glioblastoma multiforme (GBM) subtype in an individual by determining the presence of an abnormal expression of an Akt pathway gene cluster and diagnosing the cancer subtype in the individual.
EP1828209A2 Sulfonamido-macrocycles as tie2 inhibitors The invention relates to sulfonamido-macrocycles according to the general Formula (I) and the salts thereof, to pharmaceutical compositions comprising the sulfonamido-macrocycles and to a method of preparing the sulfonamido-macrocycles as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with angiopoietin and therefore influence Tie2 signalling. (I), wherein R1, R2, R4, A, X, Y, Z and m have the meaning as given in the specification and the claims.
EP1194421B1 Selective npy (y5) antagonists This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.
CN102688193A Temperature-sensitive liposome preparation of vinblastine medicament and preparation method thereof The invention relates to a temperature-sensitive liposome preparation of vinblastine medicaments and a preparation method thereof. The temperature-sensitive liposome preparation includes vinblastine medicament, temperature-sensitive phosphatide and optional long circulating material. A molar ratio of temperature-sensitive phosphatide to optional long circulating material is 70:30-92:8; and a weight ratio of vinblastine medicament to blank liposome is 1:10-1:50. The invention employs a pH gradient active drug loading method to reach an entrapment rate of 90.0-99%. The liposome preparation with heat sensitivity of the present invention can make the liposome to passively target a tumour position and release a lot of medicament simultaneously, so as to improve curative effect and reduce toxic and side effects on the whole body.
WO2009129259A3 Polymorphs of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-n-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide and methods of use therefor The invention relates to polymorphic forms of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide (referred to herein as Compound I), which has the formula: (A). The invention also relates to compositions thereof and methods for the preparation of the polymorphs of Compound I, and kits and articles of manufacture of the compositions, and methods of using the compositions to treat various diseases.
CN101225085B Phenyl urazan nitrogen nitric oxide donor 2-aniline pyrimidine derivatives, preparation method, compound containing the same and use thereof The present invention discloses a compound used as a general formula (I) of protein kinase inhibitor, the salt accepted pharmaceutically and the preparation method; wherein, X is -(CH2)m-COO-; m is equal to 1 to 5 or direct bond; Y is -(CH2)n-O- or -(CH2)n-PhO-; n is equal to1 to 10 or direct bond; the preparation method comprises a step which uses N-(5-amino-2- methyl-phenyl)-4- (3-pyridyl)-2-pyrimidinamine and general formula (II) compound as raw material synthesis. The present invention also discloses the preparation method of the compound, comprising the compound and the treatment of being used as tyrosine protein kinase inhibitor in diseases such as cancer relative to tyrosine in particular to Bcr-Abl.
CA2672534A1 Analgesic agent comprising cyclic phosphatidic acid derivative The object is to elucidate the analgesic activity of cPA, which is one of new physiological activities of cPA, and provide a novel analgesic agent. Disclosed is an analgesic agent comprising a cyclic phosphatidic acid derivative which is one of phospholipids.
CN103570531A Novel compound of antrodia cinnamomea mycelia and use thereof The invention discloses a novel compound of antrodia cinnamomea mycelia and a use thereof. The novel compound is 4-acetylantroquinonol H, 4-acetylantroquinonol I, 4-acetylantroquinonol J, 4-acetylantroquinonol K or 4-acetylantroquinonol A. The invention also discloses a pharmaceutical composition for inhibiting cancer cell growth and an inflammation reaction. The pharmaceutical composition comprises an effective amount of the novel compound.
US20100331342 Immuno Inhibitory Pyrazolone Compounds Compounds of formula (IA) or (IB) are inhibitors of CD80 and useful in immunomodulation therapy: wherein Ar represents an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group having from 5 to 10 ring atoms; R1 and R2 independently represent H, or C1-C6 alkyl; R3 represents H; F; Cl; Br; —NO2; —CN; C1-C6 alkyl optionally substituted by F or CI; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(═O)NR6R7, —NR7C(═O)R6, —NHC(═O)NR7R6 or —NHC(═S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may be interrupted by one or more —O—, —S— or —N(R8)— radicals wherein R8 represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —CF3;—OH; —SH; —NR8R8 wherein each R8 may be the same or different, or form a ring when taken together with the nitrogen to which they are attached; an ester group; or an optionally substituted aryl, aryloxy, cycloalkyl, cycloalkenyl or heterocyclic group; and R7 represents H or C1-C6 alkyl; or when taken together with the atom or atoms to which they are attached R6 and R7 form a monocyclic heterocyclic ring having 5, 6 or 7 ring atoms; and X represents a bond or a divalent radical of formula —(Z)n-(Alk)- or -(Alk)-(Z)n— wherein Z represents -0-, —S— or —NH—, Alk is as defined in relation to R6 and n is 0 or 1.
CN101422540A Medicine for curing stomatocase The invention disclose a medicine for curing canker sore, which is prepared by the following procedures of: taking asarum, plaster, typha orientalis, root of rehmannia, sanguisorba and liquorice as bulk drugs, decocting the bulk drugs by water, condensing the decocted bulk drugs into plaster, drying and grinding the plaster into medicine powder, packing the powder into a capsule; sterilizing until preparing into capsules. The medicine for curing canker sore has advantages of exact effect, rapid curing, no toxic side effect, anaphylactic reaction, low cost which can be accepted by most patients, and high curing rate of 96 percent which is tested by 276 patients suffering canker sore.
CN1732923A Ligustilide cyclodextrin or its derivatives clathrate, its preparation method and pharmaceutical formulation The invention discloses a ligustilide cyclodextrin or its derivatives inclusion compound, which comprises molecular molar ratio of 1:1-10 ligustilide and cyclodextrin or cyclodextrin derivative. The invention also discloses the process for preparing the inclusion compound, which comprises, dissolving the cyclodextrin or cyclodextrin derivatives into water, producing solution with a concentration of 5-80%, charging ligustilide, stirring, ultrasonic oscillating or grinding.
US20080108659 Poly(adp-ribose)polymerase inhibitors Compounds which inhibit the activity of poly(ADP-ribose)polymerase, compositions containing the compounds and methods of treating diseases using the compounds is disclosed.
US8071613 Anti-constipation composition An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.
WO2013021258A1 Anti-tubercular compounds The present invention relates to pharmaceutical composition comprising at least one compound of formula 1 and formula 2 for the treatment of Mycobacterial tubercular infections. More particularly, present invention discloses use of compound of formula 1 and formula 2 for the treatment of Mycobacterial tubercular infections.
CN1803788A Polymethoxylated flavone derivative with anticancer activity, its pharmaceutical composition, preparation method and application The disclosed polymethoxyflavone derivative with anticancer activity belongs to the acceptable sodium salt, potassium salt, sulfate, hydrochlorate, halogen compound or ester compound of the compound with general formula shown as (I)~(IV) or itself. This product also has small side effect with low cost.
US20060147989 administering to mammals mixtures of plant extracts from ginger, green tea, turmeric, horseradish and carriers Prophylactic and treatment methods for treatment of herpes, as well as methods for reducing or preventing the transmission of herpes. The methods comprise the step of administering to a mammal, an amount of a composition having a first ingredient obtainable from ginger; a second ingredient obtainable from green tea; an optional third ingredient obtainable from turmeric; an optional fourth ingredient obtainable from horseradish, and an acceptable carrier. When administered the composition is effective to reduce the incidence of contracting herpes, to reduce or prevent transmission of herpes, to reduce the herpes virus, or to alleviate one or more symptoms of herpes. Also disclosed are suitable formulations for delivery of the compositions for use in the methods of the invention.
WO2010049678A3 Treatment of energy utilization diseases Described are various compounds, in particular iminosugars, for the treatment of energy utilization diseases, in particular diabetes (including type 1 diabetes, type 2 diabetes and insulin resistance) and metabolic syndrome (including any disease or disorder associated therewith, for example central obesity and elevated levels of triglycerides).
CN101497622B Pyridine methyl sulfinyl imidazopyridine derivative The invention belongs to the technical field of medicine, and in particular relates to pyridinemethylsulfinyl imidazopyridine derivatives shown in a general formula (I), pharmaceutically acceptable salts of the same and isomers of the same, wherein R<1>, R<2>, R<3>, X and Y are defined in a specification. The invention also relates to a method for preparing the compounds, a pharmaceutical composition containing the compounds, and application of the compounds to preparation of medicines for treating peptic ulcer.
US6893634 Without inflammatory or other immune response side effects; injection or implantation in tissue containing cancer growth; porous cellulose sulphate and polydimethyldiallylammonium membrane; breast and/or pancreatic tumors The present invention relates to capsules encapsulating cytochrome P450 producing cells and cytochrome P450 producing retroviral packaging cells. Furthermore, the present invention relates to the treatment of cancer or any other relevant disease with said capsules and to the use of said capsules for the preparation of a pharmaceutical composition for said treatment.
CN103012405A New adenine type compound Disclosed are a new adenine type compound (shown as formula I) and salt thereof, wherein the n= 1, 2 and 3. Experimentally proved, the new adenine type compound can suppress growth of cancer cells and used for preparing antineoplastic drugs. When the R1 is H, the new adenine type compound can generate ester with inorganic acid like phosphoric acid, nitric acid and sulfuric acid, and organic acid like formic acid, acetic acid, propionic acid, oxalic acid, malonic acid, glycine, valine, maleic acid, fumaric acid, succinic acid and the like, can produce salt with acid or alkali group, and has good function of suppressing growth of the cancer cells.
US7816377 such as 1-methyl-piperidin-2-carbonsaure-[1-({1-[2-hydroxy-2-(4-phenethylcarbamoyl-thiazol-2-yl)-ethyl]-2-methyl-propyl}-methylcarbamoyl)-2-methyl-butyl]-amide, used for the treatement of adenocarcinoma The invention relates to tubulysin derivatives of general formula (II), said derivatives having a cytostatic effect.
EP2539347A2 Trimethoxyphenyl inhibitors of tyrosine kinase The present invention relates to new trimethoxyphenyl inhibitors of tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof. (I)
US20100261773 3.3.0 BICYCLIC GlyT1 INHIBITORS AND METHODS OF MAKING AND USING SAME In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
CN103405483A Oral ulcer membrane The invention relates to the field of medical instrument, and specifically provides an oral ulcer membrane. The membrane is in a three-layer structure. An upper layer and a lower layer comprise components of water-soluble chitosan and a humectant; and an interface layer comprises components of water-soluble chitosan and sesame oil. During the process of promoting healing of oral ulcer, the membrane can continuously provide nutrients for the oral ulcer, so as to enhance curative effect.
US20110158930 Method for treatment of irritable bowel syndrome A method for treatment of a patient suffering from irritable bowel syndrome with diarrhea or mixed irritable bowel syndrome, which comprises administering to the patient a therapeutically effective amount of ramosetron or a pharmaceutically acceptable salt thereof in combination with a therapeutically effective amount of polycarbophil or a pharmaceutically acceptable salt thereof.
WO2009062949A1 New polymorphic forms of n-[4-(trifluoromethyl)benzyl]-4-methoxybutyramide Crystalline polymorphic forms of a compound of formula N-[4-(trifluoromethyl)benzyl]-4-methoxybutyramide are described. The two polymorphic forms, named polymorphic Form A and polymorphic Form B, can be used in the treatment of drug addiction and alcoholism and have very good stability. Methods for preparing the polymorphic forms are also described.
US20090118355 Fluorotaxoids The invention relates to fluorinated second generation taxoid compounds, pharmaceutical formulations thereof, and their use for inhibiting the growth of cancer cells in a mammal.
CN101254165A Skin osmosis promoting absorbing agent of cryptotanshinone The invention discloses a cryptotanshinone cutaneous penetration-enhancing absorbent aiming to realize the percutaneous absorption of cryptotanshinone through carrying by 1-dodecylazacycloheptan-2-one, which is used for treating body surface suppurative inflammation of mammals caused by staphylococcus aureus, pseudomonas aeruginosa and hemolytic streptococcus. The preparation method of the absorbent comprises the steps of dissolving 2g cryptotanshinone in 100ml 65% dimethyl sulfoxide aqueous solution heated to 45 DEG C under ultrasonic vibration; adding 5g 1-dodecylazacycloheptan-2-one into the obtained mixed solution under ultrasonic vibration, and mixing; and diluting to 2mg/ml with double distilled water (using cryptotanshinone as reference). The cryptotanshinone cutaneous penetration-enhancing absorbent has the advantages of quick action, good antiphlogistic effect, low irritation, and low side effects.
US20110294815 Prostacyclin analogs This invention relates to novel prostacyclin analogs and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel prostacyclin analogs that are derivatives of treprostinil. This invention also provides compositions comprising a compound of this invention and a carrier and the use disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering analogues of prostacyclin, such as treprostinil.
CA2652783A1 Selective estrogen receptor modulators or aromatase inhibitors for treating chronic nonbacterial prostatitis A method for treatment or prevention of chronic nonbacterial prostatitis in individuals without urethral sphincter dysfunction, comprises administering an effective amount of (i) a selective estrogen receptor modulator (SERM) having estrogen antagonist effect in the prostate, (ii) an aromatase inhibitor, and/or (iii) an antiestrogen.
CN101711786A Preparation used for relieving osteoarthropathy and enhancing immunity The invention relates to a preparation used for relieving osteoarthropathy and enhancing immunity, which adopts pearl powder, a herba epimedii extract, D-aminoglucose hydrochloride and chondroitin sulfate as raw materials. The preparation is characterized by being prepared from the following raw materials proportioned by weight: 170-230g of pearl powder, 45-75g of herba epimedii extract, 85-115g of D-aminoglucose hydrochloride and 34-46g of chondroitin sulfate. After the processes of mixing, granulating, filling, or tabletting and the like, different preparations, such as capsules, tablets and the like, are prepared. The invention has the advantage that the formula has the functions of relieving the clinical symptom of the osteoarthropathy and enhancing the immunity by combining the herba epimedii extract which has the function of tonifying the insufficiency of the yang of the kidney, the D-aminoglucose hydrochloride and the chondroitin sulfate which have the functions of protecting and restoring bone joints and enhancing articular cartilages, and the pearl powder which has the function of delaying the loss of bone substances. The invention is suitable for the symptoms of bone pain, myasthenia, body contraction, hunch, easy fracture and the like caused by osteoporosis and the symptoms of constitution weakness, weary spirit, fatigue, impotence, sleep disorder and the like caused by low immunity.
CN102100699A Composition of coral calcium hydroxide and arginine and application thereof The invention discloses a composition of coral calcium hydroxide and arginine and application thereof. The composition mainly comprises the coral calcium hydroxide and the arginine, and the mass ratio of the coral calcium hydroxide to the arginine is 1:10-4:10. The composition can be prepared into granules, tablets, capsules and electuary, is used for preparing health care products for improving human immunity or preparing medicaments or health care products for treating cardio-cerebrovascular diseases. The product has obvious effects of improving human immunity and treating cardio-cerebrovascular diseases.
CN103479576A Adriamycin-wrapped polyethyleneimine-polyethylene glycol-creatine copolymer micelle and preparation method thereof The invention discloses an adriamycin-wrapped polyethyleneimine-polyethylene glycol-creatine copolymer micelle and a preparation method thereof. The preparation method comprises the following steps: under the action of pyridine, synthesizing a bicarboxyl-polyethylene glycol copolymer; synthesizing an amino-polyethylene glycol-carboxyl copolymer through amino group termination of ethylene diamine; connecting creatine and an amino group to synthesize a creatine-polyethylene alcohol-carboxyl copolymer; reacting the activated creatine-polyethylene glycol-carboxyl with polyethyleneimine to obtain a creatine-polyethylene glycol-polyethyleneimine copolymer; dialyzing to obtain the creatine-polyethylene glycol-polyethyleneimine micelle; connecting the polyethyleneimine and the creatine at the two ends of polyethylene glycol, and forming a vesicle to wrap adriamycin, with the copolymer as a drug carrier. The adriamycin is applied to clinical treatment of malignant tumors, but have relatively serious damage to normal tissues and organs of a body. The creatine is connected at one end of the polyethylene glycol, the adriamycin is wrapped inside the drug carrier, and the polyethyleneimine is connected at the other end of the polyethylene glycol, so that the stability of the adriamycin-wrapped polyethyleneimine-polyethylene glycol-creatine copolymer micelle can be improved.
EP2163249A1 Infusion solution for peripheral intravenous administration There is provided an infusion solution for peripheral intravenous administration comprising a multichamber vessel constructed in a connectable manner, which separately houses a sugar solution containing sugars, electrolytes and vitamin B1, and an amino acid solution containing amino acids, electrolytes and a sulfite, whereby the vitamin B1 and amino acids are stably maintained. In the infusion solution for peripheral intravenous administration, the sugar solution contains calcium gluconate, contains no greater than 1.4 g/L sodium lactate, has a pH of 4.0-4.7 and has a titratable acidity of 2-4, the amino acid solution contains 4.0-8.0 g/L sodium lactate, contains no calcium gluconate, has a pH of 6.8-7.2, contains free L-cysteine as cysteine and contains 0.05-0.2 g/L sodium hydrogen sulfite, and after the sugar solution and amino acid solution have been mixed, the infusion solution has a pH of 6.5-7.1 and a titratable acidity of 5-10.
WO2008012666A3 Treatment and prevention mucositis by anthocyanidin derivatives Methods for treating and preventing mucositis, in particular mucositis following the administration of chemotherapy drugs or a combination of said drugs with radiotherapy, are disclosed herein. More specifically, disclosed herein is the administration of a therapeutically effective amount of at least one of an anthocyanoside, a proanthocyanidin, or an extract containing at least one of an anthocyanoside or a proanthocyanidin for the treatment or prevention of mucositis. The therapeutically effective amount of the anthocyanoside, proanthocyanidin or extract can be administered alone or in combination with a therapeutically effective amount of at least one of an anti-inflammatory agent, immunomodulating agent, analgesic, antimicrobial agent or antifungal agent. Also disclosed herein are pharmaceutical compositions for treating and preventing mucositis.
US7238683 (Cycloalkyleneiminocarbonyl)-indanyl- or -tetrahydronaphthyl- methylamines, e.g., {(1S)-1-[(1S)-5-(4-Fluorophenyl)-2,3-dihydro-1H-inden-1-yl]-2-[(3S)-3-fluoropyrrolidin-1-yl]-2-oxoethyl}amine hydrochloride; particularly for treating type 2 diabetes The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
US20080293695 Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.
CA2685216A1 Thienopyridine and thiazolopyridine derivatives that inhibit prolyl hydroxylase activity Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure:(I) where the definitions of the variables are provided herein.
CN101804156B Preparation process and antifatigue effect of compound rhodiola root extract The invention relates to a preparation process and an antifatigue effect of a compound rhodiola root extractive, belonging to the technical field of medical product research and development. The preparation process comprises the following steps of: adding raw powder of 20-30 grams of rhodiola roots, 20-30 grams of sealwort, 10-20 grams of shizandra berry, 10-20 grams of herba epimedii and 3-5 grams of Chinese dates to 8-10 time water to soak for 4-6 hours; then extracting by heating at 10 DEG C; then carrying out ultraphonic processing for 1-1.5 hours at the temperature of 30 DEG C and the power of 80 W; then filtering by a gauze; then respectively repeating the steps for filter residues by respectively using 6 time and 4 time water once; merging three-time filter liquor; drying in vacuum; and adding 0.5-1 grams of panaxatriol saponin to obtain the compound rhodiola root extractive. The product has the main effect of antifatigue and is adapted to industrialized production.
EP2764867A1 Agents for preventing and treating disorders Involving modulation of the RYR receptors The present invention provides compounds of Formula I, (I) and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.
CN101330835A Nutritional formulations containing octenyl succinate anahydride-modified tapioca starch The present invention relates to a nutritional formulation comprising a lipid source, a carbohydrate source, a protein equivalent source, and an emulsifying agent comprising OSA-modified tapioca starch which contains less than about 0.05percent non-protein nitrogen.
US8114901 Crystalline 2,5-dione-3-(1-methyl-1H-indol-3-yl)-4-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1H-indol-3-yl]-1H-pyrrole mono-hydrochloride The present invention relates to crystalline 2,5-dione-3-(1-methyl-1H-indol-3-yl)-4-[1-(pyridin-2-yl-methyl)piperidin-4-yl]-1H-indol-3-yl]-1H-pyrrole mono-hydrochloride salt, a pharmaceutical formulation containing said salt and to methods for treating cancer and for inhibiting tumor growth using said salt.
US7482032 For preventing various kinds of damage resulting from oxidation and exposure to ultraviolet light; for use in food, cosmetics and medicine A preparation comprising the carotenoids phytoene and phytofluene in an amount which, in combination, is effective in preventing various kinds of damage resulting from oxidation and exposure to UV light is provided. The preparation is essentially colorless and may be used as a topical cosmetic or pharmaceutical preparation as well as an additive in food preparations. In addition, a method for producing substantive amounts of phytoene and phytofluene from carotenoid producing organisms is described as well.
WO2010126093A1 Agent for preventing forearm bone fracture which comprises eldecalcitol Disclosed is a pharmaceutical composition which can prevent the bone fracture in a forearm more effectively compared to conventional drugs. Specifically disclosed is a pharmaceutical composition for preventing the bone fracture in a forearm, which contains eldecalcitol.
EP1796641A1 A novel formulation, omeprazole antacid complex-immediate release for rapid and sustained suppression of gastric acid The present invention is directed to methods, kits, combinations, and compositions for treating, preventing or reducing the risk of developing a gastrointestinal disorder or disease, or the symptoms associated with, or related to a gastrointestinal disorder or disease in a subject in need thereof. In one aspect, the present invention provides a pharmaceutical composition comprising a proton pump inhibiting agent and a buffering agent for oral administration to a subject. Upon administration, the composition contacts the gastric fluid of the stomach and increases the gastric fluid pH of the stomach to a pH that substantially prevents or inhibits acid degradation of the proton pump inhibiting agent in the gastric fluid and allows a measurable serum concentration of the proton pump inhibiting agent to be absorbed into the blood serum of the subject.
WO2010031519A8 Transcutaneous compositions for specific immuno-modulatory treatment Disclosed is the use of an antigen and salicylic acid in a hydrophobic excipient as adjuvant to prepare transcutaneous compositions for specific immuno-modulatory treatment, option which is intended to generate persistent relief from allergy symptoms.
EP1588709A1 Vitamin comprising pyroloquinoline quinone and use thereof It is an object of the present invention to clarify the biochemical role of pyrroloquinoline quinone (PQQ) in living bodies by identifying an enzyme that uses PQQ as a coenzyme in mammals and then by clarifying the oxidation-reduction reaction, with which PQQ is associated as a coenzyme in living bodies. The present invention provides a method of using pyrroloquinoline quinone as a coenzyme for 2-aminoadipate 6-semialdehyde dehydrogenase.
CN102631353A Usage of toosendanin in preparation of targeted drug for resisting tumor The invention discloses usage of toosendanin in preparation of a targeted drug for resisting tumor, and discloses a human deoxycytidinekinase (dCK) which is taken as a drug target for treating related diseases of the tumor, and the function of mutant of the human dCK in development of the targeted drug for resisting the tumor.
US20090068148 Peptides of cav2.2 that inhibit pain The present invention relates to peptides of CaV2.2 and their use in the treatment of pain. The sequence of the peptides is derived from the C-terminus of CaV2.2. and is believed to inhibit the interaction of CaV2.2 with Mint1-PDZ1. The invention is related to use of this peptide to treat pain and to use of this peptide in binding reaction with int-PDZ to screen for small molecules that can inhibit pain.
US20120028942 Medicinal Cream Made Using Neomycin Sulphate, Betamethasone Valerate, And Chitosan, And A Process To Make The Same The present invention is directed to a composition for treating bacterial skin infections & skin inflammation, along with skin rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, a corticosteroid and an antibacterial active ingredient. It discloses a composition for treating bacterial skin infections & skin inflammation, along with skin rejuvenation containing a) a biopolymer in the form of chitosan, b) a combination of active pharmaceutical ingredients (APIs), neomycin sulphate & betamethasone valerate used in treating bacterial skin infections & skin inflammations, c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants and d) water. The active ingredients, namely chitosan, a corticosteroid Betamethasone Valerate, and an antibacterial agent Neomycin Sulphate, are incorporated in cream base for use in treating bacterial skin infections and skin inflammation due to allergy & itching, & wounds on human skin involving contacting human skin with the above identified composition.
CN1919209A Pharmaceutical composition for healing skin wound The invention discloses a pharmaceutical composition for healing skin wounds, which comprises the constituents of aluminium acetate basic, propylene glycol, glycerin, hydroxyethyl cellulose, synthetic borneol, sodium chloride, hydrocortisone and benzalkonium bromide. The composition can be made into dose forms of cream, paste, bandage and plaster.
US20120065166 Bone Modulators And Methods Therewith THE INVENTION RELATES TO compositions, compounds, proteins and methods of treatment therewith. Aspects of embodiments also relate to a method of treating a patient by delivering to the tissues of said patient or administering to said patient a therapeutically effective amount of one or more compounds. Aspects of embodiments also relate to a method of detecting the presence of bone disease by machine-assaying detectable serotonin. Aspects of embodiments also relate to methods of treating disease in subjects.
EP1634593A2 Hypoglycemics comprising organic zinc (II) complexes Hypoglycemics having a lower toxicity than vanadium and an adequate stability and exerting an adequate fat-soluble insulin-like effect; and medicinal preparations having an insulin-like effect and being useful as preventives and remedies for diabetes. Hypoglycemics comprising organic zinc (II) complexes which contain as the ligand selected from among ligands having pyridine ring, ligands having pyrone ring, ligands having thiazolidine ring, ligands comprising amino acids, ligands comprising 2-aminothio-phenols and ligands comprising pyrrolinedithiocarbamic acids; and medicinal preparations containing the above-described organic zinc (II) complexes which are useful as remedies for diabetes.
EP2066645A2 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions The present invention concerns novel 2 amino pyrimidine derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as harmaceuticals.
CN102846608A Pharmaceutical composition containing amlodipine and atorvastatin calcium, and preparation method thereof The invention belongs to the technical field of medical technology, and specifically relates to a pharmaceutical composition of amlodipine and atorvastatin calcium, and a preparation method thereof. The composition is composed of amlodipine or pharmaceutically acceptable salt or ester thereof, atorvastatin calcium, and pharmaceutical auxiliary materials. Atorvastatin calcium wet granulation is adopted, and amlodipine or pharmaceutically acceptable salt or ester thereof is added. The stability is good, disintegration is fast, and operation is simple. The pharmaceutical composition provides a good treatment effect in preventing or treating cardiovascular and cerebrovascular diseases.
US20120083523 Medical devices having polymeric regions with copolymers containing hydrocarbon and heteroatom-containing monomeric species According to an aspect of the present invention, implantable or insertable medical devices are provided, which contain one or more polymeric regions. These polymeric regions, in turn, contain one or more polymers, at least one of which is a copolymer that includes the following: (a) one or more unsaturated hydrocarbon monomer species and (b) one or more heteroatom-containing monomer species.
US20120093788 Protease for wound conditioning and skin care We have identified by molecular cloning a protease which originates from the larvae of Lucilia sericata and which was termed debrilase due to its activities useful for debridement of wounds. Described is a nucleic acid molecule encoding a serine protease having the ability to cleave fibrin and casein which is (a) a nucleic acid molecule encoding the serine protease comprising or consisting of the amino acid sequence of SEQ ID NO: 4 as well as to nucleic acid molecules encoding precursors or fragments of said serine protease; (b) a nucleic acid molecule comprising or consisting of the nucleotide sequence of SEQ ID NO: 3; (c) a nucleic acid molecule encoding a serine protease the amino acid sequence of which is at least 80% identical to the amino acid sequence of (a), preferably at least 85% identical, more preferably at least 90% identical, and most preferred 95% identical; (d) a nucleic acid molecule comprising or consisting of a nucleotide sequence which is at least 80% identical to the nucleotide sequence of (b), preferably at least 85% identical, more preferably at least 90% identical, and most preferred 95% identical; (e) a nucleic acid molecule which is degenerate with respect to the nucleic acid molecule of (b) or (d); or (f) a nucleic acid molecule corresponding to the nucleic acid molecule of any one of (a) to (d) wherein T is replaced by U.
CN102813739A Longevity life-prolonging tablet Disclosed is a longevity life-prolonging tablet. The longevity life-prolonging tablet is a novel product at present and is used for resisting aging and prolonging a life span of a human. The tablet is prepared by probiotics, vitamin, mineral substances and wolfberry powder. The tablet can replenish required human body nutrition, resists free radical, activates cells, eliminates infestation of the free radical for human body cells, cures and prevents disease and has special curative effect for diseases such as cancer, coronary heart disease, diabetes, autism and Alzheimer's disease. The table contains trace element selenium, vitamin E and vitamin C, the trace element selenium, the vitamin E and the vitamin C have an oxidation resistance function, and human is healthy and longevity.
CN101690744A synergistic anti-inflammatory pharmaceutical compositions and related methods using curcuminoids or methylxanthines The invention provides compositions containing a fraction isolated or derived from hops and a methylxanthine. The invention additionally provides compositions containing a fraction derived from hops and a curcuminoid. The invention also provides methods of using such compositions to reduce inflammation.
WO2006071659A1 Delivery of h2 antagonists The present invention provides improved systems and methods for the local delivery of H2 antagonists. The inventive methods include topical administration of an effective amount of a H2 antagonist encapsulated in liposomes. In certain embodiments, the H2 antagonist, for example, Cimetidine, is encapsulated into paucilamellar liposomes, such as NOVASOME® microvesicles. Also provided are pharmaceutical compositions comprising liposome-encapsulated H2 antagonists. The methods and compositions of the present invention may be used to treat any disease state or condition where local administration of H2 antagonists is beneficial.
US20080286362 mixture of non-aggregated isooctyltrimethoxysilane modified silica nanoparticle and solid bulk material in the form of a powder, containing a drug; free flowing; use in inhalation device Powder compositions exhibiting improved flow properties. The compositions generally contain a bulk solid material in the form of a powder and surface-modified nanoparticles. Methods of improving the flow of powder compositions and devices and articles made using such compositions are also disclosed.
US20090306195 Fusion Proteins of Mycobacterium Tuberculosis The present invention relates to fusion proteins containing at least two Mycobacterium species antigens. In particular, it relates to nucleic acids encoding fusion proteins that include two or more individual M. tuberculosis antigens, which increase serological sensitivity of sera from individuals infected with tuberculosis, and methods for their use in the diagnosis, treatment, and prevention of tuberculosis infection.
US20100022637 Identification of anti-cancer compounds and compounds for treating huntington's disease and methods of treatment thereof Small molecule screening via high-throughput screening (HTS) methods was employed to identify compounds useful for treating or preventing cancer (such as compounds that enable cells to overcome E6-oncoprotein-mediated drug resistance) or neurodegenerative disorders (such as Huntington's disease, HD). Compounds were identified that potentiate the lethality of anti-tumor agents as well as rescue a disease-state lethality. These compounds are acylated secondary amines referred to herein as indoxins and revertins.
CN102846652A Veterinary drug for treating viral respiratory tract disease of fowl The invention discloses a veterinary drug for treating viral respiratory tract disease of fowl, and is characterized in that the veterinary drug comprises ribavirin, ciprofloxacin lactate, aminophylline and glucose. The inventive veterinary drug can effectively treat viral respiratory tract disease of fowl, has evident curative effect and convenient application, and deserves wide generalization.
US8318683 Anti-cancer therapies Methods for the treatment of cancer are described. In particular, methods for treatment of cancer comprising administration of glufosfamide alone or in combination with another anticancer agent are disclosed.
US20130030029 Glucagon Antagonists Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof. Formula I
WO2010115556A1 Compounds and uses The invention relates to a compound having the formula of structure (I): or a pharmaceutically acceptable salt thereof, for use in treating a LH receptor-related condition.
WO2006031715A3 Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (sarms) The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I, wherein a, b, R1, R2, R3, and R4 are as defined above, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
US7101386 Patient temperature regulation method and apparatus A device and method for providing body cooling. The cooling device applies cooling to blood flowing in a vena cavae that is then distributed throughout the body. The cooling can be assisted by use of thermoregulatory drugs or warming devices to prevent shivering and vasoconstriction.
EP1115397B1 Compositions for mitigating the adverse effects of interleukin-2 A method and composition for mitigating the adverse effects of Interleukin-2 (IL-2) on a subject is disclosed. The method involves administering an amount of a leukotriene receptor antagonist to a subject exhibiting adverse pharmacological effects due to exogenous IL-2, where the amount administered to the subject is sufficient to decrease the IL-2 induced adverse effects. Also disclosed is an article of manufacturing comprising a composition of the leukotriene receptor antagonist in combination with labeling instructions for treatment. Also disclosed is a method for preparing a pharmaceutical composition.
US20070249730 Intravenous Propofol emulsion compositions having preservative efficacy The invention discloses a stable intravenous Propofol oil-in-water emulsion composition having mixed preservatives of low toxicity that is capable of withstanding accidental contamination of bacteria and fungi. The preservative system employed comprising of monoglyceryl ester of lauric acid (Monolaurin) and a member selected from (a) capric acid and/or its soluble alkaline salts or its monoglyceryl ester (Monocaprin); (b) edetate; and (c) capric acid and/or its soluble alkaline salts or its monoglyceryl ester (Monocaprin) and edetate.
US20070191485 Active oxygen scavenging composition including citrulline According to this invention, a novel anti-oxidative substance of naturally originated, with excellent ability to scavenge active oxygen species and high safety was provided. According to the present invention, citrulline was firstly exhibited to have excellent ability to scavenge active oxygen species. A novel active oxygen scavenging composition including citrulline as its effective ingredient was characterized by its excellent ability to scavenge active oxygen and high safety.
WO2007045663A3 Combination of an ati receptor antagonist and a np inhibitor fro treating ia hypertension and heartfailure The invention relates a pharmaceutical composition comprising a combination of (i) an AT1 receptor antagonist selected from the group selected from the group consisting of candesartan, eprosartan, irbesartan, losartan, saprisartan, tasosartan, telmisartan, or, in each case, a pharmaceutically acceptable salt thereof and (ii) a NEP inhibitor or a pharmaceutically acceptable salt thereof and optionally a pharmaceutically acceptable carrier and to a method for the treatment or prevention of a condition or disease selected from the group consisting of hypertension, heart failure such as (acute and chronic) congestive heart failure, left ventricular dysfunction and hypertrophic cardiomyopathy, diabetic cardiac myopathy, supraventricular and ventricular arrhythmias, atrial fibrillation, atrial flutter, detrimental vascular remodeling, myocardial infarction and its sequelae, atherosclerosis, angina (whether unstable or stable), renal insufficiency (diabetic and non- diabetic), heart failure, angina pectoris, diabetes, secondary aldosteronism, primary and secondary pulmonary hypertension, renal failure conditions, such as diabetic nephropathy, glomerulonephritis, scleroderma, glomerular sclerosis, proteinuria of primary renal disease, and also renal vascular hypertension, diabetic retinopathy, the management of other vascular disorders, such as migraine, peripheral vascular disease, Raynaud's disease, luminal hyperplasia, cognitive dysfunction (such as Alzheimer's), glaucoma and stroke, comprising administering a therapeutically effective amount of the pharmaceutical composition to a mammal in need thereof.
US20100316676 Bisphosphonate Compounds and Methods for Bone Resorption Diseases, Cancer, Bone Pain, Immune Disorders, and Infectious Diseases Bisphosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the context of functional assays such as Leishmania major farnesyl diphosphate synthase (FPPS) inhibition, Dictyostelium discoideum growth inhibition, human gamma delta T cell activation, and bone resorption. The applicability of bisphosphonate compounds in the context of parasitic infections, for example against trypanosomes, is disclosed. Further potential applications of the invention are disclosed regarding the treatment of one or more conditions such as bone resorption disorders, cancer, bone pain, infectious diseases, and in immunotherapy.
US20090306174 Novel Five-Membered Iminocyclitol Derivatives as Selective and Potent Glycosidase Inhibitors: New Structures for Antivirals and Osteoarthritis Therapeutics Novel 5-membered iminocyclitol derivatives were found to be a potent and selective inhibitors of the glycoprotein processing α- and β-glucosidase which were further found to be active antiviral agents against Japanese encephalitis virus, dengue virus serotype 2 (DEN-2), human SARS coronavirus and human β-hexosaminidase, a new target for development of osteoarthritis therapeutics.
CN102532073A Ethylene derivative serving as selective estrogen receptor modulators (SERMs) The invention provides an ethylene derivative represented by a formula I. Serving as selective estrogen receptor modulators (SERMs), the ethylene derivative can be used for preventing and/or treating diseases or disease symptoms influenced by selective estrogen receptor modulation. The formula I is shown in the specifications.
CN103601681A 3,5-pyrazoldione derivative containing exocyclic double bond structure unit and preparation method and application thereof The invention belongs to the technical field of chemical synthesis of medicines, and discloses a 3,5-pyrazoldione double bond compound of an N-substituted p-halobenzene ring with anti-tumor activity, and a synthesis method and application thereof. The compound disclosed by the invention has the structure shown by the general formula I; in the general formula I, X refers to F, Cl and Br respectively, and R1 refers to p-fluorophenyl, p-chlorphenyl, p-bromophenyl, 3-methoxy-4-hydroxyphenyl, 2,3-bis(p-methoxyphenyl), 3,4-difluorophenyl, phenylpropenyl and 2-furanpropenyl. In-vitro anti-tumor activity experiments prove that the compound has obvious effects on inhibiting and killing multiple tumor cells and can be used for preparing medicines for treating tumor diseases.
CA2318260C Solid pharmaceutical compositions containing miltefosine for oral administration in the treatment of leishmaniasis The present invention relates to new solid pharmaceutical compositions containing hexadecylphosphocholine (miltefosine) for oral administration in the treatment of leishmaniasis, a process for the manufacture of said pharmaceutical composition, a dosage scheme for oral administration of said pharmaceutical composition in the treatment of leishmaniasis, and finally a combination comprising said solid pharmaceutical composition, an antiemeticum, and/or an antidiarrhoeal.
EP1837035A1 Therapeutic agent for chronic obstructive pulmonary disease (copd), cystic fibrosis or pulmonary hypertension The present invention provides a prophylactic, therapeutic or ameliorative medicament for chronic obstructive pulmonary disease (COPD), cystic fibrosis or pulmonary hypertension. More specifically, the present invention provides: (1) a prophylactic, therapeutic or ameliorative medicament for chronic obstructive pulmonary disorder (COPD), cystic fibrosis or pulmonary hypertension, having an NF-κB decoy as the active ingredient thereof; (2) the NF-κB decoy is an oligonucleotide containing the binding sequence GGGRHTYYC (where R represents either A or G; Y represents either C or T; and H represents either A, C or T); (3) an oligonucleotide wherein the NF-κB binding sequence is GGGATTTCCC or GGGACTTTCC; (4) an oligonucleotide wherein the NF-κB decoy is represented by SEQ ID NO:3; (5) the NF-κB decoy is a double-stranded oligonucleotide; (6) the NF-κB decoy is administered in the form of a fine powder; and (7) the NF-κB decoy fine powder is a dry powder.
CN103393662A Application of Sarcaboside B to preparation of hypoglycemic medicament The invention discloses application of Sarcaboside B to the preparation of antidiabetic medicaments. The invention provides a brand new choice and thought for antidiabetic medicaments in the prior art, widens selection field of antidiabetic medicaments and contributes to the development of the technical field. The Sarcaboside B is proved to have substantial antidiabetic effects. The invention employs a compound with a clear chemical structure. The application of Sarcaboside B to the preparation of antidiabetic medicaments involved in the invention is disclosed for the first time. As the Sarcaboside B has a novel skeleton type and unimaginably strong activity in prevention and treatment of diabetes, no other compound can give any enlightenment. The invention has outstanding substantive distinguishing features and makes substantial progress in treatment of diabetes.
US20050106266 docosahexaenoic acid and a calcium compound (carbonate, hydroxide,sulfate) The present disclosure relates to novel compositions which provide improved nutritional support for premenopausal and menopausal women and/or relief from systems associated with menopause, as well as prophylactic effects, and methods for using same.
US20050158264 Sympathetic nerve-stimulating fragrant compositions Sympathetic nerve-stimulating fragrant compositions with weight-loss effects, characterized by containing one or more selected from among fennel oil, grapefruit oil, pepper oil, hyssop oil, sage oil, estragon oil, eucalyptus oil, rosemary oil, cinnamon oil, clove oil, ylang ylang oil, ginger oil, geranium oil and olibanum, or one or more from among limonene, pinene, myrcene and benzyl benzoate as the active ingredients in the oils, and preferably also containing caffeine.
EP1944030A1 Agent for treatment of schizophrenia The present invention provides an active compound (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptane-dicarboximide or a pharmaceutically acceptable salt thereof (e.g., hydrochloride) for treating symptoms of schizophrenia.
US20090149474 tert-butyl 4-[(4-chlorobenzoyl)amino]-2-(dimethylamino)-1-phenyl-1H-imidazole-5-carboxylate, used for the treatment of gastrointestinal disorders such as gastroesophageal reflux, irritable bowel syndrome, dyspepsia, diarrhea and for the inhibition of transient lower esophageal sphincter relaxations The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.
WO2011026536A1 Novel therapeutic concepts for treating fibromyalgia The invention relates to novel concepts for the prophylactic and/or therapeutic (curative) treatment of diseases, in particular fibromyalgia, that occur in human or veterinary medicine, are caused by faulty control of nociception, and/or can be treated by inhibiting nociception.
WO2014069667A1 Agent for preventing or improving decline in brain function An objection of the present invention is to provide an agent for preventing or improving decline in brain function such as decreased perception ability, decreased memory learning ability, decreased thinking ability, decreased concentration, decreased attention, decreased judgment ability, depression, and decreased exercise performance caused thereby. According to the present invention, an agent for protecting brain neuronal cells, comprising citrulline or a salt thereof and citicoline or a salt thereof as active ingredients as well as an agent for preventing or improving decline in brain function, comprising citrulline or a salt thereof and citicoline or a salt thereof as active ingredients is provided.
US20110237638 Metronidazole-based dermatological foam and emulsions for the preparation thereof Oil-in-water emulsions expandable into stable foams having diminished inhibitor of skin breathing and useful for the treatment of dermatological conditions/afflictions, e.g., rosacea, advantageously contain: (a) 72% to 76% of water; (b) 0.1% to 5% of a gelling agent for the aqueous phase of the emulsion; (c) 0.75% to 2% of metronidazole; (d) 5% to 10% of mineral oil; (e) 0.5% to 10% of a surfactant; (f) 0.5% to 5% of a fatty acid; (g) 0% to 4% of a metronidazole absorption promoter (c); and (h) 0.1% to 5% of a preservative selected from the group consisting of methylparaben, propylparaben, phenoxyethanol and mixtures thereof.
WO2009091831A1 Compound forms and uses thereof The present invention provides, among other things, forms of a compound of formula 1. In some embodiments, the present invention provides salt forms and/or crystal forms. In some embodiments, the present invention provides solid forms. The present invention also provides methods of making and using provided forms.
WO2012150042A1 Compounds and methods for the identification of histone demethylase interacting molecules and for the purification of histone demethylase proteins The present invention relates to immobilization compounds, immobilization products and preparations thereof as well as methods and uses for the identification of histone demethylase interacting compounds or for the purification or identification of histone demethylase proteins.
US7906128 Controlling parasites in animals by administerinng sodium channel activators The present invention provides an effective method and composition for the prevention, amelioration or control of external parasites on a human or animal via the administration of a prophylactically, therapeutically or pharmaceutically effective amount of a neuronal sodium channel antagonist to a human or animal in need thereof.
US20120003320 Particles which are surface coated with hyaluronan or one of the derivatives thereof and the use of same as biological vectors for active substances Particles comprising a core based on at least one biodegradable organosoluble polymer. At least a part of the surface of the particles is coated with at least one hyaluronan or a derivative thereof, the hyaluronan being a water-soluble, amphiphilic hyaluronan of which the carboxylic functions are in part transformed to form hydrophobic groups.
CN103211795A Cefaclor film-controlled slow-release pellet capsule The invention relates to a cefaclor film-controlled slow-release pellet capsule. A slow-release film of the cefaclor film-controlled slow-release pellet utilizes a mixture of aqueous dispersion Eurdragit RL 30D and Eurdragit RS 30D as a film-formation material, wherein a weight ratio of Eurdragit RL 30D to Eurdragit RS 30D in the mixture is 4: 1. A pellet core of the cefaclor film-controlled slow-release pellet contains sodium carboxymethyl starch having high expansibility, and also contains pharmaceutically-acceptable common excipients for the slow-release pellet, wherein preferably, the excipients comprise microcrystalline cellulose and lactose, and the pellet core comprises 5 to 20wt% of the sodium carboxymethyl starch. The slow-release film comprises the mixture of Eurdragit RL 30D and Eurdragit RS 30D, triethyl citrate as a plasticizer, and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit RL 30D to Eurdragit RS 30D to triethyl citrate to talcum powder is 24: 6: 2: 4 and a film weight increasing ratio is in a range of 23 to 40%. The cefaclor film-controlled slow-release pellet comprises the pellet core containing sodium carboxymethyl starch having high water expansibility and thus after absorbing water, the cefaclor film-controlled slow-release pellet obviously expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the cefaclor film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.
CN102503896A Methylacryloyl-benzimidazole (sulfur) ketone derivative and application of serving as antibacterial agent thereof The invention discloses a novel methylacryloyl-benzimidazole (sulfur) ketone derivative, a preparation method for the compound and an application of the compound serving as an antibacterial agent. The compound has the structure shown in the following general formula (I) in the specification, wherein R and Y in the general formula (I) have meanings as shown in the specification.
EP2598500A1 Compositions and methods for inhibition of the jak pathway Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.
US20100204304 NOGO Receptor Binding Protein The invention provides Sp35 polypeptides and fusion proteins thereof, Sp35 antibodies and antigen-binding fragments thereof and nucleic acids encoding the same. The invention also provides compositions comprising, and methods for making and using, such Sp35 antibodies, antigen-binding fragments thereof, Sp35 polypeptides and fusion proteins thereof.
CN101822685A Application of asiaticoside The invention discloses application of asiaticoside in preparing medicaments for treating erectile dysfunction, wherein the unit dosage of the asiaticoside is 5-800mg. Pharmacological tests and clinical experiments show that the medicament of the invention has the advantages of little side effects, wide therapeutic window, and the like, cannot lead to after effect to a sufferer after being taken, and has the characteristic of the natural medicament and very good pharmacological actions.
US20110097420 Cement products and methods of making and using the same Disclosed are cement products, methods of forming cement using the cement product, and methods of using the cement product in orthopedic and dental applications. Generally, the disclosed cement product includes a first component comprising a polymerizable resin comprising ethylenic unsaturated double bond, a second component comprising a compound comprising more than one type of amine selected from the group consisting of primary amines, secondary amines, tertiary amines and quaternary amines, and, optionally, the cement product includes a bioactive component to promote bone formation.
US8377645 Unc-33 like phosphoprotein (ULIP) polypeptide for generating antibodies for use in diagnosis, preventnion and treatment of neurodegenerative and neoplastic disorders A purified polypeptide, designated ULIP6, comprising the amino acid sequence SEQ ID No. 2 or an epitopic fragment of said polypeptide, comprising the sequence SEQ ID No. 4, is provided along with its nucleic acid sequences. In addition, antibodies to the polypeptide and methods of diagnosing paraneoplastic neurological syndromes and/or for the early diagnosis of the formation of cancerous tumors are also provided.
CN102225139B Chenshu invigorating spleen paste and its preparation method The invention discloses a Chenshu invigorating spleen paste and its preparation method. The Chenshu invigorating spleen paste is prepared by the following raw materials by weight ratio: 15 to 25g of banksia rose, 15 to 25g of root of large-flowered skullcap, 15 to 25g of rhizoma atractylodis, 50 to 70g of haw, 5 to 15g of notopterygium root, 15 to 25g of dried orange peel, 50 to 70g of medicated leaven, 15 to 25g of bighead atractylodes rhizome, 15 to 25g of pogostemon, 30 to 50g of radix paeoniae rubrathe, 15 to 25g of betel nut, 30 to 50g of Poria cocos, 15 to 25g of radix Saposhnikoviae, 15 to 25g of combined spicebush, 5 to 15g of borneol and 30 to 50g of lotus leaf. The Chenshu invigorating spleen paste is capable of treating abdominal distention and little appetite, as well as constipation caused by spleen deficiency and dampness-heat, and also used for promoting gastrointestinal motility and assisting an absorption of medicines and food, so that the paste provided in the invention has good functions of invigorating spleen, removing dampness and relieving dyspepsia.
CN1651420A Dehydro methyl abietate furazan derivative, its synthesis method and use A methyl deoxyabietate-furazan derivative series, their synthesizing process and their application are disclosed. Said series is composed of 9-methyl carbonyldeoxyabietate-furazan oxide, 9-methyl carbonyldeoxyabietate-furazan, 12,13-methyl deoxyabietate-furazan oxide, 12,13-methyl deoxyabietate-furazan, and 12-bromo-13,14-methyl deoxyabietate-furazan oxide.
US20130004563 Multiparticulate s-adenosylmethionine compositions and related methods Multiparticulate compositions having S-adenosylmethionine an active ingredient are disclosed. The multiparticulates have spheroidal core comprising S-adenosylmethionine, microcrystalline cellulose, and hydroxypropyl methylcellulose; a sub-coat comprising hydroxypropyl methyl cellulose on the spheroidal core; and an enteric coat on the sub-coated spheroidal core. The average diameter of the particulates is about 0.1-3 mm. Other aspects of the invention include methods of making and methods of using the multiparticulate compositions.
US7141658 Nucleotide sequences in the rpoB gene of spirochetes code for the beta subunit of the bacterial RNA polymerase; amplification, sequencing and comparison; complexing with genetic probes The invention concerns single stranded oligonucleotides comprising a sequence of at least 12 consecutive nucleotide motifs contained in one of the sequences SEQ ID NO: 1 to SEQ ID NO: 4 wherein “n” represents an identical or different nucleotide selected among inosine or an equimolar mixture of 4 different nucleotides selected among a, t, c or g, and among oligonucleotides complementary thereto. The invention also concerns using the oligonucleotides to detect bacteria of the Spirochaetales order. The invention is based on the use of specifically defined sequences in the rpoB gene of spirochetes coding for the beta subunit of the bacterial RNA polymerase.
CN102048792A Medicinal composition for preventing and treating heat rash and preparation method thereof The invention relates to a medicinal spray for preventing and treating heat rash and a preparation method thereof. The medicinal composition comprises the extract of parslane herb, honeysuckle flower and Chinese mugwort leaf, and mirabilite, has high safety, is convenient to use and suitable for children, and can effectively prevent and treat the heat rash.
EP2426132A1 Process for preparing 14-hydroxycodeinone from thebaine The present invention relates to a process for preparing 14-hydroxycodeinone from a thebaine composition.
EP1515961A1 N,n-disubstituted diazocycloalkanes useful for the treatment of cns disorders due to serotonergic dysfunction N,N-Disubstituted diazocycloalkanes of the formula (I): (R<1> = halogen, R<2> = (C3-C8)-cycloalkyl, R<3> = (C1-C4)-alkoxy or (C1-C4)-haloalkoxy group, m is 1 or 2, n is 1 or 2) have affinity for serotoninergic receptors. These compounds and their enantiomers, diastereoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts are useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptor. 1,4-Disubstituted-piperazines (n = 1) are preferred. R<1> is preferably F in the 2-position, R<2> is preferably cyclohexyl, and R<3> is preferably a methoxy or 2,2,2-trifluoroethyl group. Preferably, m = 1.
CN101837022A American cockroach medicinal composition for curing gastritis and peptic ulcers and preparation method thereof The invention discloses an American cockroach medicinal composition for curing gastritis and peptic ulcers. The medicinal composition is mainly prepared from an active ingredient mixture prepared by mixing an American cockroach extract and gypsum. The weight part ratio of the American cockroach extract to the gypsum is equal to 0.8-1. 2g : 2.5-40g. A preparation method of the American cockroach medicinal composition for curing the gastritis and the peptic ulcers comprises the following steps of: preparing the American cockroach extract, mixing active ingredients, and preparing medicaments. The medicinal composition has simple preparation method, fully exerts effects of the American cockroach extract, and effectively improves curative effects on the gastritis and the peptic ulcers.
US20080275044 Vanilloid receptor 1 antagonists; reducing a phenyl or 3-pyridyl carboxylic acid or ester to an alcohol, aziding, reduction to a primary amine, amidation with a (3-fluoro-4-methylsulfonamido)phenyl acetic acid; 2-(3-Fluoro-4-(methylsulfonamido)phenyl)-N-(substituted phenyl or pyrid-3-yl) acetamides Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical compositions containing such compounds, a process for the producing such compounds, and the use thereof to treat or inhibit pain and/or various other disorders or conditions.
US20120058208 Synergistic Composition for Enhancing Bioavailability of Curcumin The present disclosure relates to a composition to enhance the bioavailability of curcumin. In one embodiment, a composition comprising plant extracts of curcumin, vanilla and ginger, wherein the extracts of ginger and vanilla are rich in gingerol and vanillin respectively, is provided. In other embodiments, curcumin, and one or more items selected from the group of vanilla, ginger and capsaicin is provided.
US20090069403 Composition and method for reducing allergen This invention relates to an allergen-reducing composition comprising a hydroxyproline derivative, a polymer thereof, or a salt of such a derivative or polymer, which is capable of reducing the allergenicity of mites, pollens, or other allergens and is capable of imparting functions of reducing allergenicity to fibers or textiles such as a carpet, a tatami mat, a bed cloth, a curtain, clothing, a stuffed animal, a mask, a filter material, or a dust bag for an electric vacuum cleaner without discoloration; and a method for reducing allergens using such composition.
US7279480 Hexahydropyridazine-3-carboxylic acid hydrazide and hydrazone derivatives, combinatorial libraries containing same, pharmaceutical compositions containing same and methods of preparation The present invention discloses and claims hexahydropyridazine-3-carboxylic acid hydrazides and hydrazones of formula (I) as inhibitors of proteases and kinases, and methods of using said compounds of formula (I) for the prevention or treatment of certain cardiovascular, central nervous system, inflammatory, and bone diseases as well as infectious diseases and certain cancers. Combinatorial libraries of the compounds of formula (I), pharmaceutical compositions, and methods for the preparation of combinatorial libraries and the compounds of formula (I) are also disclosed and claimed.
US7250262 For the diagnosis and treatment of patients with disorders including anemias The present invention relates to methods for the diagnosis and treatment of hematological disorders. Specifically, the present invention identifies the differential expression of 131, 148, 199, 12303, 13906, 15513, 17822, 302, 5677, 194, 14393, 28059, 7366, 12212, 1981, 261, 12416, 270, 1410, 137, 1871, 13051, 1847, 1849, 15402, 340, 10217, 837, 1761, 8990 and 13249 genes in tissues relating to hematological disorders sensation, relative to their expression in normal, or non-hematological disorders disease states, and/or in response to manipulations relevant to hematological disorders. The present invention describes methods for the diagnostic evaluation and prognosis of various hematological disorders, and for the identification of subjects exhibiting a predisposition to such conditions. The invention also provides methods for identifying a compound capable of modulating hematological disorders. The present invention also provides methods for the identification and therapeutic use of compounds as treatments of hematological disorders.
EP1237877B1 Carboxamide-substituted benzimidazol derivatives, methods for the production thereof and their use as medicaments The invention relates to carboxamide-substituted benzimidazol derivatives of general formula (I), wherein R1 represents an optionally substituted residue from the group C¿1?-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, phenyl-C1-C4-alkyl, heterocyclyl, heterocyclyl-C1-C4-alkyl; R?2¿ represents -C(=NH)NH¿2?, -CH2-NH2; R?3¿ represents an optionally substituted residue from the group C¿1?-C6 alkyl, C1-C6 hydroxyalkyl, C1-C4 alkoxy-C1-C4-alkyl, heterocyclyl, heterocyclyl-C1-C4-alkyl, heterocyclyl-C2-C4-alkenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl-C1-C4-alkyl, naphthyl-C1-C4-alkyl, and; R?4¿ represents hydrogen and an optionally substituted C¿1?-C6 alkyl, optionally provided in the form of their tautomers, racemates, enantiomers, diastereomers, mixtures thereof and pharmacologically safe acid addition salts thereof. The invention also relates to methods for the producing said carboxamide-substituted benzimidazol derivatives and to their use as medicaments having a tryptase-inhibiting effect. The invention additionally relates to so-called prodrugs , wherein R?2¿ represents C(=NR7)NH2 and intermediate products, wherein R2 represents -CN.
WO2008129319A1 Salts of oxadiazole derivatives as dgat inhibitors Sodium, magnesium, tert -butylammonium salt, tris( hydroxymethyl)methylammonium, triethanolammonium, diethanolammonium, ethanolammonium, methylethanolammonium, diethylammonium and nicotinamide salts of a compound of formula (I) are provided, which compounds inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity: Formula (I) wherein R 1 is phenyl optionally substituted with 1, 2 or 3 substituents independently selected from fluoro, chloro, bromo, trifluoromethyl, methoxy, difluoromethoxy, trifluoromethoxy, cyano, methyl and ethyl; R A is hydrogen or methyl; p is 0 or 1; with the proviso that the salt of formula (I) is not sodium ( trans -4-{4-[({5-[(2,4,5- trifluorophenyl) amino]-1,3,4-oxadiazol-2-yl} carbonyl)amino]phenyl}c yclohexyl)acetate; together with processes for preparing such compounds, their utility in treating clinical conditions associated with obesity, methods for their therapeutic use and pharmaceutical compositions containing them.
CN101618133B Application of yang-reinforcing kidney-protecting medicine in preparing medicine preventing and treating osteoporosis The invention discloses an application of a yang-reinforcing kidney-protecting medicine in preparing a medicine preventing and treating osteoporosis. The yang-reinforcing kidney-protecting medicine can improve the bone density of an osteoporosis model animal, increases the bone and mineral contents, prevents the drop of the sexual hormone level of an old-aged animal and a person and the like, andhas the effects of resisting senility, enhancing the sexual gland function and the like.
US20100113415 Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.
US6900231 Aminopyridyl-substituted phenyl acetamides as protease inhibitors Phenyl acetamide compounds are described, including compounds of or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.
WO2008146035A1 Combination of chk and parp inhibitors for the treatment of cancers A combination, comprising a checkpoint kinase (CHK) inhibitor, or a pharmaceutically acceptable salt thereof, and a poly (ADP-ribose)polymerase (PARP) inhibitor, or a pharmaceutically acceptable salt thereof is described.
US20100092459 Protein Complex and Uses The present invention relates to a complex comprising two or more of the proteins S6K2, PKCε and B-Raf. The invention also relates to antibodies that specifically bind to the complex, inhibitors of the complex and uses of the antibodies, inhibitors and complex in diagnosing and preventing chemoresistance in a patient.
CN101585770B Caffeic acid diester compounds and preparation method thereof, and application thereof in preparing medicine for curing thrombus The invention discloses caffeic acid diester compounds of formula (I) and prepartion method thereof, and application of preparing medicine for curing thrombus, experments show that the invention synthesized caffeic acid diester compounds has strong inhibition function to platelet aggregation induced by ADP, comparison of 50% aggregation inhibition concentration shows that, the invention provided caffeic acid diester compounds has better inhibition function to platelet aggregation than caffeic acid and acetylsalicylic acid, the caffeic acid diester compounds obtained by condensation of caffeicacid and acetylsalicylic acid has synergistic function with less clinical dosage, reduced untoward effect. The invention provided method for preparing caffeic acid diester compounds uses microwave reaction that reduces reaction time and improves reaction efficiency, and the cost is reduced, the invention also has excellent operability and certain protection function to environment.
US20060079503 Thiazolidinones and the use therof as polo-like kinase inhibitors Thiazolidones of general formula I in which R1, R2, R3, X and Y have the meanings that are indicated in the description, their production and use as inhibitors of polo-like kinases (PLK) for treating various diseases as well as intermediate products for the production of thiazolidones are described.
WO2006014790A3 Compositions containing policosanol and omega-3 fatty acids and their pharmaceutical uses A composition is provided which contains policosanol and omega-3 fatty acids and which may be used for treating and or reducing hypercholesterolemic diseases, total cholesterol, LDL-cholesterol, LDL/HDL ratio, triglycerides, coronary heart disease (heart attacks and strokes), sudden cardiac death, ventricular fibrillation, tachycardia, hypertension, inflammation, thrombosis, deep-vein thrombosis, stroke, macular degeneration, autoimmune and/or immunoregulatory diseases, cardiovascular diseases, anxiety, depression and/or neurodegenerative disorders, and/or raise HDL cholesterol in humans and animals. The method comprises administering policosanol and omega-3 fatty acids which together effectively lower the LDL/HDL cholesterol ratio. Typically, the administered composition includes about 0.1-10:1 parts by weight of policosanol to omega-3 fatty acids.
US7119180 Halogenation with a diphenylhalosulfonimide, deblocking the protected hydroxyl group; optional esterification or addition salt formation A subject of the invention is a process for the preparation of the compounds of formula (I): Wherein the substituents are defined as in the application. The compounds of this invention exhibit antibiotic properties.
US20050004227 Cell growth inhibitor The present invention revealed that AT-264 suppresses cell growth through its inhibitory effect on PepT1 activity. Furthermore, as a result of examining whether AT-264 comprises the effect of inhibiting the cell growth of human pancreatic cancer cell line AsPC-1, the present invention revealed that cell growth is similarly suppressed. These findings show that cell growth can be suppressed by inhibiting the activity of peptide transporters. Suppression of peptide transporter activity can be considered to be an important indicator in the development of growth inhibitors for cancer cells and such.
EP2051979A2 Polymorphic forms of rosiglitazone base The present invention relates to novel polymorphic forms of rosiglitazone base, as well as to a process for their preparation and pharmaceutical formulations containing it. The present polymorphic forms of rosiglitazone base are characterized by small average particle sizes and high solubility bestowing the compounds an improved bioavilability.
US20130116290 Use of Dipeptidyl Peptidase IV Effectors for Normalizing the Blood Glucose Level in Mammals The present invention comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to lower elevated post-prandial and basal blood glucose levels in mammalian organisms. The invention further comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to increase the half-life of incretins in vivo.
CN103073451A Histone deacetylase inhibitor The invention provides a histone deacetylase (HDAC) inhibitor compound (E)-4-(3-hydroxyamino-3-oxo-1-propenyl)-2-methoxyphenol-4-((5,5,8,8-tetramethyl-5,6,7,8-tertralin-2-yl)carbamoyl)benzoate. The compound has obvious inhibitory effects on HDACs and growth and proliferation of human leukemia U937 cells, and the inhibitory effects of the compound are substantially superior to those of the commonly used HDAC inhibitor trichostatin A (TSA). The invention further provides a preparation method and a process route for the compound.
US7964734 Raloxifene acid addition salts and/or solvates thereof, improved method for purification of said raloxifene acid addition salts and/or solvates thereof and pharmaceutical compositions comprising these Raloxifene acid addition salts or solvates thereof, having improved dissolution properties in media comprising hydrochloric acid are described, compared with similar preparations based on raloxifene or raloxifene hydrochloride. The disclosed acid addition salts or solvates thereof show an improved bioavailability in media comprising hydrochloric acid, such as the gastric juice. The acid addition salts or solvates thereof are addition salts or solvates of raloxifene and a pharmaceutical acceptable acid selected among succinic acid, lactic acid, malonic acid or sulphuric acid. Further, crystalline forms of the raloxifene salts and solvates thereof are disclosed. The raloxifene acid addition salts and/or solvates thereof are useful for the preparation of pharmaceutical composition for oral administration capable of fast and reliable release of the active ingredients in the stomach of the patient, in particular for the treatment of cancer or osteoporosis, or for inhibiting cartilage degradation. A new method for preparation of raloxifene lactate is also disclosed.
CN102895245A Compound trimethoprim and doxycycline hydrochloride nanoemulsion preparation and preparation method thereof The invention discloses a compound trimethoprim and doxycycline hydrochloride nanoemulsion preparation. The nanoemulsion preparation is of an oil-in-water type, and the grain size of the nanoemulsion preparation is between 1nm and 100nm. The nanoemulsion preparation is prepared from the following raw materials in weight percentage: 0.01-1.75 percent of trimethoprim, 0.04-6.99 percent of doxycycline hydrochloride, 21.8-35.7 percent of surfactant, 7.94-11.9 percent of cosurfactant, 3.49-4.76 percent of oil and the balance of distilled water. The compound preparation is an oil-in-water type nanoemulsion; the compound preparation is flaxen and transparent in appearance; the grain size of the compound preparation is between 1nm and 100nm, so that the stability is high; and the trimethoprim and the doxycycline hydrochloride in the preparation show up an obvious synergistic effect, The compound nanoemulsion preparation has the advantages of safety, broad spectrum, high efficiency, targeting and slow release.
EP1811998B1 Triazoles useful as inhibitors of protein kinases The present invention relates to inhibitors of proteins kinases of formula (I). The invention also provides pharmaceuticals compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
US20090005455 (R,S)-1-[2-oxido-(dimethylamino)-1-(4-methoxyphenyl)ethyl]-cyclohexanol (venlafaxine N-oxide); depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine Embodiments of the invention relate to a compound of formula (1), or a tautomer, stereoisomer, hydrate, or solvate thereof, wherein R1 is H or CH3. Other embodiments of the invention relate to a pharmaceutical composition containing these compound, to methods for preparing these compounds, and to methods for preparing compositions containing these compounds. Yet other embodiments of the invention relate to the uses of these compounds and compositions containing it, such as for the manufacture of medicaments and pharmaceutical compositions for treating a condition chosen from depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine and hot flashes.
EP2282743A1 Sulfated unsaturated disaccharidic chondroitin sulfate in connective tissue protection and repair The present invention generally relates to the protection and repair of connective tissues. In particular, the present invention relates to the use of chondroitin sulfates and its derivatives in connective tissue protection and repair. The present inventors have found that unsaturated disaccharidic chondroitin sulfate can be used for the preparation of a composition to develop, protect and/or repair connective tissues. This allows it for example to treat or prevent osteoarthritis or rheumatoid arthritis, and/or the symptoms thereof as well as to treat or prevent signs of skin ageing such as the appearance of wrinkles effectively.
US7749971 Such as Hurler syndrome and Batten by administering an aminoglycosidesuch as gentamicin, G418, hygromycin B, paromomycin, tobramycin, lividomycin A, amikacin, sisomycin, or neomycin, optionally in combination with an enzyme effective for enzyme replacement therapy, a polyionic compound or gene therapy The present invention provides a method of treating lysosomal storage diseases such as Hurler syndrome and Batten disease in individuals in need of such treatment, comprising the step of administering to said individuals a therapeutically effective dose of an aminoglycoside. In addition, this method may further comprise treating the individual with enzyme replacement therapy. Furthermore, the present invention provides method of pharmacologically suppressing premature stop mutations in an individual with these lysosomal storage diseases, comprising the step of administering to said individual a pharmacologically effective dose of an aminoglycoside.
WO2008044848A1 A composition comprising an extract of rhei rhizoma or physcion compound isolated therefrom for treating or preventing cognitive dysfunction and the use thereof The present invention relates to a composition comprising an extract of Rhei rhizoma or physdon compound isolated therefrom showing potent inhibiting effect on the aggregation and toxicity of beta-amyloid and recovering activity of memory learning disorder confirmed by Y maze study and Passive Avoidance study. Therefore it can be used as the therapeutics or health care food for treating and preventingcognitive function disorder with safe.
WO2012034969A1 Gt aptamer oligonucleotides and use thereof as antitumor agents The invention relates to aptamer oligonucleotide having a GT sequence, and derivatives thereof, having a well-defined length, and their use as antitumor agents alone or in association with antitumor agents currently in therapeutic use. The oligonucleotide according to the invention may, in addition to a therapeutic use, have a diagnostic use in that it is capable of detecting proteins of the eEF1A family.
US20110027394 Cross-Linked Biopolymers, Related Compounds and Methods of Use The present invention provides stabilized oil-in-water emulsions with an extended range of chemical, thermal and/or mechanical stabilities, and method(s) for their preparation. Such preparations provide an environmentally-protective biopolymer component exhibiting improved adherence to the dispersed phase, reducing or eliminating dissociation therefrom under such conditions, for use in the context of a range of food, pharmaceutical, personal care, health care, cosmetic and other end-use applications.
US8609653 Azaindole compounds and methods for treating HIV Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
US7129231 Regulation of intracellular glucocorticoid concentrations This invention relates to the interconversion of inactive 11-keto steroids with their active 11B-hydroxy equivalents, to methods by which the conversion of the inactive to the active form may be controlled, and to useful therapeutic effects which may be obtained as a result of such control. More specifically, but not exclusively, the invention is concerned with interconversion between cortisone and cortisol in humans.
WO2007061868A2 Treatment of stereotypic, self-injurious and compulsive behaviors using specific serotonin reuptake inhibitors and antagonists of nmda receptors A combination of a specific serotonin reuptake inhibitor (SSRI) and an NMDA receptor antagonist can be used in methods of treatment, for reducing the frequency of stereotypic behaviors in animals and for reducing the frequency of analogous compulsive behaviors in humans, for example, those that have been said to be a manifestation of, or related to, obsessive-compulsive disorder.
CN101224222A Cydiodine buccal tablet and preparing method thereof The invention discloses a cydiodine buccal tablet and a preparation method thereof, which is characterized in that the invention comprises the following components by weight proportion: 0.05-8 percent of cydiodine inclusion complex, 0.20-8 percent of sildenafil inclusion complex, 75.0-96 percent of cane sugar, 0.01-5.0 percent of hydroxypropyl methyl cellulose, 0.20-5.0 percent of magnesium stearate, 0.01-10.0 percent of povidone. The invention well solves the stability problem of drug guest molecules, namely, molecular iodine. The drug guest molecules, that is, molecular iodine or menthol, is included and composited by main molecular, namely beta-cyclodextrin, and specific high molecular, namely, povidone, which can further enhance solubility and dissolution rate of drugs, prevent volatile components escape, improve stability, cover inherent bad smell of some drugs and decrease irritation. The invention well solves the stability problem of iodine preparation and menthol; therefore the novel inclusion technique has practical significance and more important value.
EP1795181A1 Cosmetic and pharmaceutical uses of the dipeptide tyrosine-arginine in combination with niacinamide as substance P antagonist Use of a combination (C1) comprising niacinamide and tyrosine-arginine dipeptide or its derivatives to prevent and/or decrease cutaneous rednesses and/or swellings. - ACTIVITY : Dermatological; Antipruritic; Analgesic; Antiallergic; Antiinflammatory; Antipsoriatic; Virucide. The ability of the combination to treat edema was tested. The results showed that the combination of the niacinamide and the dipeptide exhibited an improved effect than that of the two components alone. - MECHANISM OF ACTION : Substance P antagonist.
CN1876162A Plaster for treating orthopaedic diseases and its preparation process Disclosed is a medical ointment for treating orthopaedic diseases and its preparation process, which is prepared mainly from 10-20 parts of Schizonepeta tenuifolia, Kusnezoff monkshood root, hooked uncaria, pubescent angelica root, futokadsura stem, eucommia bark, safflower, cortex acanthopanacis, Chinese flowering quince, green tangerine orange peel, notopterygium root, Sichuan aconite root, large-leaf gentian root, fresh ginger, buthus martensi karsch, spicebush root, oriental wormwood, donkey-hide gelatin, 5-8 parts of centipede and calomel, 450-550 parts of red lead and 1000 parts of vegetable oil.
US20080253989 Neuron Regeneration The invention provides a gene silencing molecule, which is adapted to down-regulate expression of a gene encoding a peptide involved with the Rho-A inhibitory pathway. The gene silencing molecule is used to promote neuron survival and axon regeneration in the central nervous system (CNS). The invention also provides compositions and methods of using same to improve neural survival and promote axonal growth.
US20110136772 Sugar coatings and methods therefor Compositions particularly useful as coatings for solid dosage forms of therapeutic agents are provided, as are solid dosage forms comprising such coatings, processes for preparing such solid dosage forms, and the products of those processes. The coating compositions generally provide excellent strength and resistance to cracking, even when applied to flexible/swellable tablet cores such as hydrogel-type cores. The compositions also exhibit excellent odor-blocking characteristics.
WO2010107765A1 Bicyclic compounds as inhibitors of diacylglycerol acyltransferase The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below : formula (I).
US7696365 Heterocyclic compounds useful as malonyl-CoA decarboxylase inhibitors The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.
US20100267721 Heterocyclic H3 Antagonists Compound of formula (I) wherein W, X, Y, Z is —C(R′)═ or N; R1 is hydrogen or alkyl, V is N or C (i.e. carbon), A is a bond or an alkylene linker with 1 to 3 carbon atoms, with the proviso that when A is a bond, V must be CH, R is ethyl, propyl, a branched C3-6 alkyl or a cyclic C3-8 alkyl, m and n is 1-3, D is heteroaryl optionally substituted with halogen, hydroxy, cyano, alkyl, cycloalkyl, alkoxy, —(CH2)o—(C═O)p—NR2R3, or D is aryl optionally substituted with one or more of the groups independently selected from hydrogen, halogen, hydroxy, cyano, alkyl, cycloalkyl, haloalkyl, alkoxy, haloalkoxy, alkylsulfonyl, alkylsulfinyl, heterocyclyl, heterocyclylalkyl, heterocyclyl-alkoxy, heterocyclylcarbonyl, alkylcarbonyl, alkoxycarbonyl, alkylcarboxy, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonylamino, alkylcarbonylaminoalkyl, arylcarbonylamino, aryl-carbonylaminoalkyl, heteroarylcarbonylamino or heteroarylcarbonylaminoalkyl, —(CH2)0—(C═O)p—NR2R3, wherein o is 0-3, p is 0 or 1, and R2 and R3 independently are hydrogen, alkyl or cycloalkyl; or R2 and R3, can together with the attached nitrogen form a heterocyclyl group, and salts and solvates thereof have binding affinity for the histamine H3 receptor.
CN102920894A Medicament for treating arthralgia and myalgia and preparation method thereof The invention discloses a medicament for treating arthralgia and myalgia, which comprises sargentgloryvine stem, radix gaultheriae, mulberry twig, pubescent holly root, aloe, China fir leaf, salt and liquorice. The medicament has the effects of relaxing tendons and activating collaterals, invigorating circulation of vital energy and activating blood, and is used for treating arthralgia and myalgia caused by various reasons, such as arthralgia, inhibited bending and stretching and limbs anesthesia. The medicament is simple in preparation method and low in cost, has great social and economical values, and can help people get rid of arthralgia and myalgia.
WO2013175297A1 Salts of saxagliptin with organic acids The invention relates to organic salts of Saxagliptin and processes for their preparation.
US20100204340 Orally bioavailable stilbenoids- compositions and therapeutic applications thereof A novel, bioavailable and safe stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 with an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis, and nutraceutical and cosmeceutical compositions comprising 3,5-dimethoxy-3,4′-dihydroxystilbene useful for anti-obesity and anti-cellulite therapy, are disclosed. Further the enhanced SIRT-1 activation ability of 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 and 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are disclosed. The enhancement of SIRT-1 polypeptide activity of the said compounds is unexpectedly much higher than resveratrol or its natural analog pterostilbene. Sirtuin modulating compositions comprising an orally bioavailable SIRT-1 enhancing compounds (i) 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I and (ii) 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are also disclosed. An additional embodiment, also discloses the enhanced anti-Propionibacterium acnes activity of 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I and compositions thereof.
CN103284964A Children zinc gluconate-milk composition freeze-dried oral disintegrating tablet and preparation method thereof The invention provides a children zinc gluconate-milk composition. The composition comprises the following ingredients in percentage by weight: 1.0-1.6% of zinc gluconate, 1.3-2.4% of mannitol, 2-4% of gelatin, 90-97% of milk powder, and 0.1-0.15% of sucralose. The invention also provides a children zinc gluconate-milk composition freeze-dried oral disintegrating tablet which is prepared from the composition. The freeze-dried oral disintegrating tablet is simple in ingredients, less in intestinal residue, complete to absorb, good in taste, and especially suitable for an infant to take, and does not need water and chewing when taken, the disintegrating time of the freeze-dried oral disintegrating table in an oral cavity of a human body is not more than 2 seconds.
EP1918281A1 Phenylamino-substituted piperidine compounds, their preparation and use as medicaments The present invention relates to phenylamino-substituted piperidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.
US20080045566 6-substituted isoquinoline derivatives The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R4 is H or (C1-6)alkyl, optionally substituted with halogen, (C3-7)cycloalkyl, (C6-10)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C6-10)aryl and heterocyclic ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy or halogen; R5 is H or (C1-4)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.
CN101863867A Derivatives of flavonoids compounds and preparation method and application thereof The invention discloses derivatives of flavonoids compounds and a preparation method and application thereof. The general formula of the compounds is shown in the formula I in the specification. The preparation method provided by the invention is characterized in that corresponding phenol 1 (such as p-chlorophenol, alpha-naphthol and the like) is stirred in iced water solution with the ratio of phenol to acetic oxide to sodium hydroxide being 1:2-3:2-3 to obtain acetylate; anhydrous aluminium chloride and sodium chloride are melted and stirred for 2h to obtain corresponding rearranged phenol; the rearranged phenol reacts with different acyl chloride in the presence of pyridine to obtain substituted phenylethyl benzoate; the substituted phenylethyl benzoate is heated by anhydrous pyridine and potassium hydroxide to obtain corresponding different substituted dibenzoylmethane; and the different substituted dibenzoylmethane flows back and is stirred in glacial acetic acid and concentrated sulfuric acid to obtain the structural formula I. The compounds have good anti-tumor effect and have important practical value and application prospect in the field of preparing anti-tumor drugs.
EP2607366A1 Glycerol phenyl butyrate esters The present invention refers to Glycerol Phenyl Butyrate Esters, including esters and amides, their stereoisomers, enantiomers, racemates as well as the acids, bases or salts thereof, medicaments comprising them, as well as their use in cancer therapy and other pharmaceutical applications. wherein one of R1, R2 or R3 is
CN101711252A heterocyclic spiro-compounds The patent application relates to new heterocyclic compounds of the general formula (I), in which R, R<1>, R<2>, Q, T, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
CN101884681A Cake for treating supramammarici erosion The invention discloses a method for preparing a cake for treating supramammarici erosion. The method comprises the steps of: drying mume fruit for 10 to 20 minutes, taking the dried mume fruit out, grinding the dried mume fruit, calomel and single powder, adding saliva until the powder is not bright, and bouncing the powder to form a circular cake, namely the finished cake. By utilizing the method, the supramammarici erosion can be cured by applying the cake for several hours.
CN101890000A Application of gambogic acid as inhibitor of heat shock protein 90 The invention discloses the application of gambogic acid as an inhibitor of heat shock protein 90, relates to the gambogic acid and provides the application of the gambogic acid in preparing the inhibitor of the heat shock protein 90. The name of the gambogic acid is (z)-methyl-3-pentenyl)-; 1,5-dimethylene-1,3,11-trihydrotris-furo (3,4-g) pyrano (3,2-b) anthranone-1-crotonic acid, the molecular formula of the ambogic acid is CH38H44O8, the optical activity of the ambogic acid is minus 685 degrees, the gambogic acid is insoluble in water and well soluble in organic solvents such as methyl alcohol and the like. The gambogic acid is capable of inhibiting the ATP enzymatic activity of the heat shock protein 90 and degrading the client protein of the heat shock protein 90, and has wide application in preparing drugs for treating various diseases caused by the abnormal activity of the heat shock protein 90.
WO2007107346A1 Substituted indazole derivatives, their manufacture and use as pharmaceutical agents Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
US20090048347 Topical anesthetic for rapid local anesthesia and method of applying a topical anesthetic The invention relates to a drug delivery system for the topical administration of anesthetic agents. For example, a topical anesthetic for rapid local anesthesia is provided. The topical anesthetic includes an anesthetic, volatile and non-volatile solvents, and an optional thickener. In addition, a method is taught for applying the topical anesthetic to the face of a patient without occlusion. The anesthetic is applied topically to an area for injection such that the dermatological procedure (cosmetic injections) can be performed in fifteen minutes.
CN102120747A Water-soluble photostable silver (I) complex and preparation method and application thereof The invention relates to transition metal coordination polymer, in particular to a water-soluble photostable silver (I) complex with a bacteriostatic effect and a preparation method thereof. A chemical formula of the complex is [Ag8(L)2(DMF)2]infinite, wherein L is a 3,4,5,6-tetrafluorophthalatedicarboxyl anionic ligand, and DMF is N,N-dimethylformamide. The complex is synthesized in methanol and DMF solution by a solvent volatilization method by taking silver nitrate and 3,4,5,6-tetrafluorophthalic acid as reaction raw materials. The synthesis method is mild in conditions, high in yield and repeatability, and is convenient to operate. A complex crystal sample has high bacteriostatic activity to staphylococcus aureus, Escherichia coli and bacillus subtilis, high water solubility and photostability, is convenient to store and transport, and can be applied to the fields of medical treatment and life science; and the minimal inhibitory concentration is in the range of 0.5 to 2mu g/mL.
CN102499944A Nanometer silver antibiotic and antiviral compound liquid and its preparation method and products The invention discloses a nanometer silver antibiotic and antiviral compound liquid and its preparation method and products. The compound liquid is prepared by using materials of nanometer silver colloid and polyvinylpyrrolidone, wherein the weight of polyvinylpyrrolidone is 0.01-40% of the weight of the nanometer silver colloid. The invention solves problem that the silver nanometer particles have poor affinity with cells and partially coagulate in long-term preservation when the nanometer silver colloid is in antibiotic and antiviral practical application; the nanometer silver antibiotic and antiviral compound liquid has characteristics of practicability, economy, intoxicity and high efficiency.
WO2009154230A1 Prophylactic/ameliorating or therapeutic agent for non-alcoholic steatohepatitis Disclosed are: a safe and highly effective prophylactic/ameliorating or therapeutic agent for NASH; and use of the agent. The prophylactic/ameliorating or therapeutic agent for NASH comprises a combination of at least one component selected from the group consisting of ω3PUFAs, a pharmaceutically acceptable salt thereof and an ester thereof and a PDE4 inhibitor as active ingredients.
WO2012131638A1 Functional food for male use including muirapuamine and yohimbine The present application relates to and claims the following: A functional food preparation comprising at least one dairy product and a composition of substances of vegetable origin, said composition being characterized by a combination of muirapuamine and yohimbine, wherein said combination is present in a concentration which ranges from 0. 01% to 2% by weight, relative to the total weight of the preparation. The following is also encompassed by the claims: Use of said composition in the prevention and treatment of disorders of the ma urogenital system correlated to andropause, such as bladder problems, urinary disorders, prostatic hypertrophy, prostate cancer and sexual disorders, preferably low libido or erectile dysfunctions.
CN101418334B Diterpenes diterpenoids natural product inhibitor for main protease of coronaviruses such as SARS and screen method thereof The invention provides a method for screening a diterpene natural product inhibitor from Rabdosia henryi (Hemsl.) Hara on the basis of in vitro inhibitory activity screening and a crystal structure of coronavirus main proteinase such as SARS, TGEV and AIBV. People find that a compound provided with the following structural formula can effectively inhibit the activity of the coronavirus main proteinase.
CN101897667A Doxorubicin hydrochloride liposome injection and preparation technology thereof The invention discloses a doxorubicin hydrochloride liposome injection and a preparation technology thereof. The injection comprises the following components by weight percent: 0.05-0.5% of doxorubicin hydrochloride, 0.025-3% of hydrogenated soybean phosphatidylcholine, 0.001-1.5% of cholesterol, 0.01-1% of PEG-lipid, 0.0025-2.5% of organic acid or ammonium sulfate, 2.8-20% of sugar, 0.1-10% of buffering agent and the balance water for injection. The preparation technology comprises the following steps: 1) freeze-drying lipid phase; 2) hydrating lipid phase; 3) straightening the granules of lipid phase; 4) forming transmembrane gradient inside and outside phospholipid membrane; 5) loading medicine with liposome; and 6) degerming, subpackaging and storing.
CN1895264B Medicinal use of quercetin-3-0-beta-D-glucancoside An application of the quercetol-3-0-beta-D-glucoside in preparing the medicines for treating cerebral anoxia and ischemia, and thrombosis is disclosed. Said quercetol-3- 0-beta-D-glucoside is prepared from rutine by semi-synthesis method with high output.
US20070197470 Use of n-acetyl-d-aminogylcosamine in preparation of drugs for modulating microorganisms on mucous membrane The present invention has disclosed a use of N-acetyl-D-glucosamine in the preparation of a medicament for regulating microecological balance of mucocutaneous membrane. N-acetyl-D-glucosamine has functions of promoting bacteria and cellular redistribution and against allochthonous flora colonization. Preparations comprising N-acetyl-D-glucosamine as main active substance are able to be used for regulating microecological balance of mucocutaneous membrane, and have advantages of significant therapeutic effects, simple manufacture, nonirritant, non-pollution, etc.
CN103446178A Application of lauromacrogol in preparation of medicine for treating pyogenic granuloma The invention discloses a novel application of lauromacrogol, namely, treating pyogenic granuloma. The lauromacrogol can be used as a raw material for preparing a medicine for treating pyogenic granuloma. According to the novel application of lauromacrogol, new application of an approved drug is realized; the novel application cannot be rationally presumed or forecasted by the technician in the field through the original application (treating esophageal varix); such discovery brings important application value.
US20110124718 Reduction Of Acetaminophen Toxicity By Dietary Milk Thistle Extract The present invention is directed to the reduction of acetaminophen toxicity by dietary milk thistle extract. Milk thistle has been reported to have protective effects on the liver and to greatly improve its function. It is typically used to treat liver cirrhosis, chronic hepatitis (liver inflammation), and toxin-induced liver damage. The present invention, for the first time, combines milk thistle and acetaminophen in a unique and novel way to provide single dosages containing both ingredients, whether dispensed in a liquid suspension, chewable tablets, coated caplets, gelcaps, geltabs, and suppositories.
CN101416945A Preparation method of azithromycin fine granule The invention pertains to a preparation method adopting a spray-drying method to encapsulate drugs into miniature capsule fine granules, more particularly relates to the preparation of azithromycin fine granules. The preparation method comprises the steps that: (1) poly-acrylic acid resin is soaked in an organic solvent, stirred, dissolved and prepared into a poly-acrylic acid resin solution after being filtered by a mesh sieve; (2) azithromycin material is added into the poly-acrylic acid resin solution obtained from Step 1), thus obtaining a mixed material; (3) the mixed material of Step (2) is treated with spray-drying, and miniature capsules are collected; and (4) the miniature capsules obtained from the Step (3) are added with a sweet food additive, mixed evenly, dried and prepared into granules. The preparation method prepares the azithromycin material solution into the miniature capsules by the way of spray-drying and solves the disagreeable taste effect caused by the bitterness of azithromycin preparations by sweet layers wrapping the outer layers of the miniature capsules. The solving of the taste of the azithromycin preparations cause the granules to be convenient for users to take, especially for children and patients with chronic diseases and needing to take the granules for a long term.
US20050090489 An alpha hydroxy acid or a retinoid as a bacterial fermentation product of a novel Streptomyces strain; topical antiwrinkle agents A composition containing a peripheral benzodiazepine receptor ligand for topical use in the treatment of cutaneous stress.
US20130023508 Hyaluronic acid based copolymers Hyaluronic acid (HA) conjugates or crosslinked HAs compositions for coating an implantable device are provided. The implantable device can be used for treating a disorder such as atherosclerosis, thrombosis, restenosis, high cholesterol, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, and combinations thereof.
CN1593412A Method for preparing nimodipine carrying float sustained release mini capsule The invention discloses a method for preparing nimodipine carrying float sustained release mini capsule which consists of, preparing the aqueous solution of sodium bicarbonate - sodium alginate - konjac glucomannan, preparing nimodipine solid dispersion, charging the nimodipine solid dispersion into the aqueous solution of sodium bicarbonate - sodium alginate - konjac glucomannan and mixing, charging the mixed liquid into the aqueous CaCl2 solution of acidic chitosan with micro droplets, washing the spherical articles, freezing and drying.
CN2712349Y Subcutaneous implantable sustained-release silica gel rod for antipsychotics The utility model discloses a subcutaneous implantable sustained-release silica gel rod for antipsychotics, which is characterized in that the subcutaneous implantable sustained-release silica gel rod for antipsychotics comprises a minor segment of medical silicone tube. Antipsychotics having long therapeutic effect, high titer and low therapeutic dose is filled in the medical silicone tube; both ends of the silicone tube are sealed by medical adhesive. The subcutaneous implantable sustained-release silica gel rod for antipsychotics can be used for adopting trochars having small notches with the puncturing and the guiding to be implanted on the inner side of the arm, near the groin position of the abdominal wall, or at the loose position of the hypodermis of the inner side of the thigh after the satisfactory effect on the acute treatment is obtained; 6-7 sustained-release silica gel rods of the utility model can be implanted one time. The subcutaneous implantable sustained-release silica gel rod for antipsychotics has simple configuration, convenient manufacture and operation, enduring therapeutic effect, and economy. The therapeutic effect can persist for 5-6 years by one time implanting; the medicine can be slowly released via the medical adhesive of both ends of the silicone tube, which ensures the effective haemoconcentration to achieve the purpose of maintaining the therapy. The subcutaneous implantable sustained-release silica gel rod for antipsychotics is suitable for the invalids having various schizophrenosis and repeatedly paroxysmal manic symptom.
CN101444554B Snake-fat ointment and preparation method thereof The invention discloses snake-fat ointment and a preparation method thereof, relating to an itching-relieving skin protectant. The snake-fat ointment which takes snake oil as the main material and the preparation method thereof are provided. Material components of the snake-fat ointment comprises snake oil, hexadecanol, nipagin, chlorhexidine, borax, hydrolyzed pearl solution, 2,6- butylated hydroxy toluene, panaxoside, vitamin A, vitamin D, vitamin E, K12, medicinal oils and stroma. The preparation method comprises the following steps: (1) the snake oil, the hexadecanol, single gangliosides,stearic acid, octodecyl alcohol, chrismaline, vitamin A, vitamin D, vitamin E are heated and molten to obtain dissolution liquid; (2) the nipagin, the chlorhexidine and borneol are taken and added with alcohol for dissolution, and menthol, camphor and wintergreen oil are added, stirred and dissolved each other; (3) the panaxoside, the 2,6- butylated hydroxy toluene, the K12, the glycerin and the borax are taken and added with water and dissolved, and the hydrolyzed pearl solution is then added, the solution obtained by the step (2) is added during the stirring, then mixed and heated till boiling, the dissolution liquid is added after cooling, and the product is finally obtained by stirring till emulsification.
US20090311291 Condoms with lubricant compositions and packaging providing enhanced functionality The present disclosure provides improved packaged condoms that enable the use of a large quantity of a composition inside the condom. In addition, a sufficient quantity of certain spermicidal and/or microbicidal compositions is provided for efficient inactivation of sperm and pathogens. The present disclosure also provides condoms with reduced tendency to slip or break. Compositions associated with different surfaces of the condom can be effectively segregated to their intended condom surface according to the present disclosure.
US7317040 Nitric oxide synthase inhibitor phosphate salt A compound of formula (I): namely (2S)-2-amino-4-{[2-(ethanimidoylamino)ethyl]thio}butanoic acid, compound with phosphoric acid, or a solvate or physiologically functional derivative thereof, is useful as a relatively non-hygroscopic selective inhibitor of inducible nitric oxide synthase.
WO2014140671A1 New arylaminoalcohol derivatives with antiplasmodial activity The present invention relates to new arylaminoalcohol derivatives of formula (I), and to a method for the preparation of such compounds: The invention also relates to the use of these compounds as medicaments, and in particular for the prevention and/or the treatment of parasitic diseases caused by apicomplexan parasites such as malaria and toxoplasmosis. Finally, the invention relates to pharmaceutical compositions containing such compounds of formula (I) as active principles.
CN103751797A Enzyme-controlled release pharmaceutic preparation with dual effects, preparation method and application thereof The invention relates to a pharmaceutic preparation, in particular relates to an enzyme-controlled release pharmaceutic preparation with dual effects, a preparation method and application thereof, and belongs to the technical field of pharmacy. The enzyme-controlled release pharmaceutic preparation comprises parts A, B, C and D, wherein the part A is gold nanorods; the part B is polyethylene glycol; the part C is matrix metalloproteinase specific recognition enzyme; the part D is methylprednisolone. According to the preparation method, a steroidal anti-inflammatory medicament, namely, methylprednisolone, is connected to the surfaces of polyethylene glycol-gold nanorods by using substrate matrix metalloproteinase specific recognition enzyme as a link arm, so as to obtain a methylprednisolone-substrate matrix metalloproteinase specific recognition enzyme-polyethylene glycol-gold nanorods targeted delivery system, and as a result, the enzyme-controlled release pharmaceutic preparation with dual effects of pharmaceutical therapy and thermal therapy is realized.
US20070264198 Tumor necrosis agent The present invention relates to novel drugs (pharmaceuticals) such as tumor necrosis agents, uses of substances having tumor necrosis effect for production of tumor necrosis agents, methods of screening substances having tumor necrosis effect, and methods of treating or improving tumor(s), particularly methods of necrotizing tumor(s). The invention further provides active ingredients that are used in drugs suitable for destroying or damaging tumor(s) effectively and selectively to animal needing treatment of tumor(s), particularly humans (patients), and enables the use of the active ingredients in drugs, the screening of such active ingredients and the therapy of tumor(s) using such drugs.
WO2012030513A2 Methods of treating bacterial infections through pulmonary delivery of fusidic acid Methods for the treatment of bacterial infections in the respiratory system of a subject, such as the lungs of a subject, using fusidic acid alone or in combination with a second bacterial agent such as tobramycin, amikacin, fosfomycin or levofloxacin are described.
US8673917 2-heteroaryl-pyrrolo [3,4-C]pyrrole derivatives, and use thereof as SCD inhibitors The invention relates to compounds of the formula (I), where the groups R1, M, A, B, D, L, and R have the specified meanings, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treating metabolic syndrome, insulin resistance, obesity, and diabetes.
WO2007023507A2 Oxazolidinones bearing antimicrobial activity composition and methods of preparation The present invention provides compounds of Formula (I) having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention provides novel oxazolidinone derivatives, processes for making compounds as well as antimicrobial pharmaceutical compositions containing said derivatives as active ingredients and methods of treating microbial infections with the said derivatives. Formula (I): wherein Q is formula (II): or formula (III).
WO2012175587A3 Crystalline cefoperazone intermediate, process for its preparation and pharmaceutical use thereof The present invention relates to a crystalline form of an intermediate for cefoperazone of formula (1 ) and to a process for the preparation thereof by enzymatic condensation of a 3'-thiosubstituted β-lactam nucleus with a phenylglycine derivative.
WO2007033515A1 Oral formulation containing moxifloxacin and its preparation method An oral tablet formulation of moxifloxacin or its salts and/or hydrates, comprises at least one film-forming material used for coating the intermediate particles. Said film-forming material may be one or more of hydroxypropyl methylcellulose, hydroxyethyl methylcellulose, methylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, sodium carboxymethycellulose, polyacrylic resins, polyethylene glycol, polyvinylpyrrolidone vinylacetate copolymer, PVA-PEG graft copolymer, carbopol, gelatin, poloxamer, polyvinylpyrrolidone. Preparation of said formulation comprises: mixing or granulating moxifloxacin blended with excipients, coating the intermediate granular with the film- forming material, then compressing the mixture. The invented tablet formulation has a prolonged shelf life and rapid dissolution.
CN1751684A Novel form of Asimidazole for treating nasal polyls or its disease An inhalation, tablet, or capsule made of astemizole or the medicine containing astemizole for treating nasal polyp and its disease is disclosed.
CN1927050B DHA microcapsule food additives, DHA soft capsule health product and uses thereof The invention relates to a kind of DHA microcapsule food additive and DHA microcapsule functional food, both of which are made up of core material and capsule wall material. What's unique about the products is that the core material contains the docosahexaenoic acid and/or the compound which docosahexaenoic acid is its component fatty acid. Besides, the ratio of docosahexaenoic acid and icosapentaenoic acid is 7 or higher. The products are low in EPA, pollutants, and offensive smell of fish. So they are quite safe to serve as the additive or functional food for infants and children.
CA2851623A1 5,7-substituted-imidazo[1,2-c]pyrimidines Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
CN1887898A Amino acid as chemical modifier for ursolic acid The amino acid chemically modified ursolic acid is one semi-synthesized product, and is prepared through the following steps: 1. reaction between ursolic acid and acetic anhydride to produce acetoxy ursolic acid; 2. reaction between acetoxy ursolic acid and oxalyl chloride and further reaction with corresponding amino acid to produce intermediate products; and 3. hydrolyzing the intermediate products to obtain amino acid chemically modified ursolic acids as the target compounds. The present invention obtains serial ursolic acid analogs, which are proved through pharmacological tests to have HELA human body cervical carcinoma cell inhibiting activity higher than that of ursolic acid.
CN101318985A Preparation method for ursolic acid, produced products and application thereof The invention discloses a method for preparing ursolic acid and a product and an application thereof. The method comprises the following steps that: loquat leaves are pulverized, added with 95 percent ethanol and subjected to ultrasonic extraction for 0.5 to 2 hours; an extractant is filtered by a micromembrane; a filtrate is separated by an ultrafiltration membrane and a nanofiltration membrane to produce a mixed solution of the ethanol and the ursolic acid; the ethanol is reclaimed, and the ursolic acid is obtained; the obtained ursolic acid is mixed with grosvener siraitia and honey to prepare grosvener siraitia honey cream. The invention adopts a method of combining ultrasonic extraction and membrane separation and purification, and extracts the ursolic acid from the loquat leaves; the method has relatively simple process flow, small loss of effective compositions, an ursolic acid yield of more than 75 percent, small ethanol amount and low energy consumption, thereby reducing extraction cost; and the prepared grosvener siraitia honey cream has the faint scent and sweetness of the grosvener siraitia and the light fragrance, fresh and sweet taste and mellowness of the honey, and has the functions of sedation, heat-clearing and lung-moistening, intestine moistening, defaecation and sleep improvement, thereby becoming a high-quality health-care product integrating nutrition and health care.
CN102000147A Medicament formula and preparation thereof for preventing and curing altitude reaction and coronary heart disease The invention relates to a medicament formula and a preparation thereof for preventing and curing an altitude reaction and a coronary heart disease. The medicament formula comprises 10 to 40g of rhodiola rosea, 60 to 150g of salvia miltiorrhiza, 1 to 5g of ginkgo biloba extract and 0.3 to 1.5g of artificial musk or borneol. The preparation comprises oral solid preparations of dripping pills, troches, capsulas, granules, pills, powder, and the like. The preparation method of dripping pills is characterized by extracting salvianolic acid B of salvia miltiorrhiza extract by adopting a method combining alcohol extraction and ethyl acetate extraction, the purifying method adopts macroporous adsorbent resins, and an eluent is 20% to 60% ethanol. The extraction of salidroside of rhodiola rosea extract adopts 30 to 90% ethanol for heating and backflow, the purifying method adopts the macroporous adsorbent resins, and the eluent is 10 to 50% ethanol. A salvia miltiorrhiza purified matter (salvianolic acid B), a rhodiola rosea purified matter (high-purity salidroside), the ginkgo biloba extract and the artificial musk or borneol are mixed with PEG (polyethyleneglycol) 4000 and PEG 6000 which are 0.5-3 times the amount of the salvia miltiorrhiza purified matter (salvianolic acid B), the rhodiola rosea purified matter (high-purity salidroside), the ginkgo biloba extract and the artificial musk or borneol, the , the mixture is heated for fusion and kept at 60 to 80 DEG C, and the mixture is dropped to a coolant, condensated, screened and dried to obtain the preparation.
WO2010086964A1 Combination therapy for treating cancer Disclosed is a combination therapy for potentiating the effect of inhibiting tumor growth and/or metastasis wherein an inhibitor of plasminogen activator inhibitor-1 is combined with a cytotoxic agent or a cell growth inhibitor.
WO2013168000A1 Compositions and methods for the treatment of severe pain The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for the treatment of severe pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of chronic pain, generalized pain disorders, leukemia, cancer, chronic pain, chemotherapy induced pain, epilepsy, migraine, neuropathic pain, post herpetic neuralgia, neuralgia, pain, drug addiction, detoxification of drugs, Alzheimer's disease, multiple sclerosis, multiple sclerosis restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, amyotrophic lateral sclerosis (ALS), convulsions, partial seizures, mood-stabilizing agent and bipolar disorder.
US20120115842 Substituted Oxindole Derivatives, Medicaments Containing Said Derivatives and Use Thereof The invention relates to novel oxindole derivatives of general formula (I), wherein substituents A, B, X and Y are defined as in claim 1, medicaments containing said derivatives, and the use thereof in the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
WO2009143153A1 Substituted pyrrolidine amides as modulators of the histamine h3 receptor Certain substituted pyrrolidine amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
US20050026938 Purine inhibitors of protein kinases, G proteins and polymerases The present invention relates to purine analogs that inhibit, inter alia, protein kinases, G-proteins and polymerases. In addition, the present invention relates to methods of using such purine analogs to inhibit protein kinases, G-proteins, polymerases and other cellular processes and to treat cellular proliferative diseases.
CN1891210A Ranitidine bismuth citrate dispersible tablet, and its preparing method The present invention relates to a bismuth citrate ranitidine dispersion tablet and its preparation method. Said tablet preparation contains bismuth citrate ranitidine compound and medicinal auxiliary material. Its preparation method includes the following steps: (1), pulverization and mesh screening, respectively pulverizing bismuth citrate ranitidine main medicines and medicinal auxiliary material, mesh screening by means of sieve with 80-100 meshes; (2), making soft material, uniformly mixing the above-mentioned all the medicinal materials and adding ethyl alcohol or aqueous solution of povidone K30 as adhesive, and making them into soft material; (3), granulation and granule finishing, using sieve with 20-30 meshes to make granulation, drying for 2hr at 50-80 deg.C, then finishing granules by using sieve with 20-30 meshes; and (4), content determination, tabletting so as to obtain the invented finished product.
US7868041 prodrugs of gabapentin and pregabalin, such as 2-[1-[[[(2R)-6-oxooxan-2-yl]oxycarbonylamino]methyl]cyclohexyl]aceticacid, used for for treating epilepsy, depression, anxiety, psychosis, brain disorders, neurodegenerative diseases, pain, inflammatory disease, gastrointestinal disorders or drug abuse The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.
US20120171308 Antioxidant Complex, Cosmetic and Pharmaceutical Compositions Containing Said Complex, and Use of Said Complex The present application describes an antioxidant complex having a synergistic effect between its ingredients. Said mixture comprises: a) vitamin E and/or derivatives thereof; b) green tea extract and/or derivatives thereof; and c) cacao extract. Examples of cosmetic and pharmaceutical compositions comprising said antioxidant complex and a physiologically acceptable carrier are also described. The antioxidant complex of the present invention, as well as the aforementioned compositions, aid in preventing and protecting against cell and skin damages resulting from the action of free radicals, and also provide DNA, protein and cell membrane protection.
US20120296263 Topical aminolevulinic acid-photodynamic therapy for the treatment of acne vulgaris Light treatments of sebaceous gland disorders with 5-aminolevulinic acid and photodynamic therapy are disclosed. A preferred treatment includes topical application of 5-aminolevulinic acid to the skin followed by light exposures with repeated treatment at various intervals. At low doses of ALA and photodynamic therapy (PDT) in single or multiple treatments, improvement in the sebaceous gland disorder, e.g., acne, provides the discovery that diminishment in sebum secretion and the eradication of bacteria occurs. At high doses of ALA and a single high energy PDT treatment, permanent changes to the sebaceous gland and sebum secretion have been discovered.
WO2011146511A1 A crystalline form of (r)-7-chloro-n-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.
CN102641259A Application of glaucocalyxin A in preparation of anticoagulation medicaments The invention relates to application of glaucocalyxin A and particularly relates to application of glaucocalyxin A in preparation of anticoagulation medicaments. The glaucocalyxin A can be used for remarkably prolonging the capillary coagulation time and tail tip bleeding time of mice, and remarkably prolonging the thrombin time (TT), prothrombin time (PT), activated partial thromboplastin time (APTT) and plasma recalcification time (PRT) of the mice. The glaucocalyxin A can be used for remarkably prolonging the TT, APTT and PRT for domestic rabbits in vitro. The results of in-vivo-administration anticoagulation experiments prove that the glaucocalyxin A can be used for remarkably prolonging the APTT and PRT of the mice, thereby prompting that the glaucocalyxin A can be used for inhibiting the generation of fibrin by disturbing intrinsic coagulation factor activity; and the remarkable prolonging of the TT proves the inhibition of transformation from fibrinogen to fibrin. The results of the in-vivo-administration anticoagulation experiments also prove that the glaucocalyxin A has a certain inhibition effect on extrinsic coagulation pathways since the glaucocalyxin A can be used for remarkably prolonging the PT. The results of in-vitro experiments prove that the glaucocalyxin A can be used for remarkably prolonging the APTT, PT and PRT, but has no obvious effects on the PT, thereby proving that the glaucocalyxin A realizes the anticoagulation effect in vitro mainly through inhibiting intrinsic coagulation pathways.
WO2010136705A1 Pharmaceutical antitumor composition including a cdk inhibitor and a cell-growth inhibitor The invention relates to the field of cancer therapy and specifically to a pharmaceutical composition having an antitumor effect and including at least one CDK inhibitor selected from indirubin-3'–monoxime and certain selected purine derivatives and at least one cell-growth inhibitor. The invention also relates to the combination of at least one CDK inhibitor selected from indirubin-3'–monoxime and certain selected purine derivatives, and at least one cell-growth inhibitor having synergetic antitumor effects for use as a drug for treating neoplastic diseases.
CN103288823A N,N'-aryl substituted urea compound and application thereof The invention mainly relates to an N,N'-aryl substituted urea compound and an application thereof. The N,N'-aryl substituted urea compound is a compound shown in the formula I or a salt formed by the compound and a medicinal acid or alkali. The provided compound has the strong inhibitory activity for receptor protein kinases which comprise VEGFR2 (Endothelial Growth Factor Receptor 2), RGFR1 (Fibroblast Growth Factor Receptor 1) and PDGFR Alpha (Platelet Derived Growth Factor Receptor Alpha) and associated with the neogenesis of three kinds of tumor tissue blood vessels. Thus, the N,N'-aryl substituted urea compound can be used as a multi-target kinase inhibitor which is developed into a targeted anti-tumor medicine for treating solid tumors.
US20060094686 Use of corrinoids for application in skin diseases The use of compounds of the formula I in which R stands for CN, OH, CH3 or H2O, for building up and improving the resistance of the skin is claimed. The compounds are suitable in particular for preventive treatment in cases of predisposition to chronic skin diseases, for the prevention and treatment of allergic skin reactions, for the treatment of acute skin injuries, for example burns and wounds, as well as in aging of the skin, and in the treatment of degenerate cells, such as in cancers, benign and/or malignant tumours.
WO2011113608A1 Esterified polysaccharide osmotic agents The invention relates to esterified polysaccharide osmotic agents, to the use thereof, to a method for the preparation thereof and to compounds containing said osmotic agents.
CN101559107A Chinese materia medica preparation for treating folliculitis The invention belongs to a Chinese materia medica preparation for treating folliculitis. The preparation is made from the following materials: cocklebur fruit, alum, wild chrysanthemum flower, flavescent sophora root, cnidium fruit and broom cypress fruit. The Chinese materia medica preparation has scientific formula, low cost, short course of treatment, quick effect, high curative ratio and no side effect on human body.
CN103316351A Electrostatic spinning complex loaded with two drugs The invention discloses an electrostatic spinning complex loaded with two drugs, which is prepared by the following steps of: dissolving 50-99 weight parts of water-soluble polymer with good biocompatibility and 0.1-20 weight parts of hydrophilic drug in distilled water to obtain mixed liquid; dispersing 1-50 weight parts of degradable polymeric micelle loaded with a hydrophobic drug in distilled water to obtain dispersion liquid; mixing the mixed liquid and the dispersion liquid to obtain spinning liquid; and performing electrostatic spinning on the spinning liquid, and drying in vacuum to obtain the electrostatic spinning complex loaded with two drugs. The electrostatic spinning complex is loaded with a hydrophilic drug in electrostatic spinning and is also loaded with a hydrophobic drug in the electrostatic spinning polymeric micelle, so that the hydrophilic drug and the hydrophobic drug can be released at different times and a better treatment or restoration effect is realized.
EP1697346A1 Crystalline form of 2-{ 4-[3-(4-chloro-2-fluorophenyl)-4-pyrimidin-4-yl-1h-pyrazol-5-yl]piperidin-1-yl} -2-oxoethanol Crystalline form of the p38 kinase inhibitor 2-{4-[3-(4-chloro-2-fluorophenyl)-4-pyrimidin-4-yl-lH-pyrazol-5-yl]piperidin-1-yl}-2-oxoethanol can be used, is provided. The crystalline form is a hydrated crystalline form. Also provided are combinations and pharmaceutical compositions comprising the crystalline form, process for preparing the crystalline form and for preparing compositions comprising the crystalline form, in methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline form of 1.
EP2581084A1 Solid dispersion comprising triazole compound A solid dispersion comprising a poorly soluble pharmaceutical compound, such as 3-methoxy-1,5-bis(4-methoxyphenyl)- 1H-1,2,4-triazole, which has excellent ease of handling and stability is provided. The solid dispersion comprises a polymeric carrier (for example, a polymer selected from a group consisting of polyvinylpyrrolidone and copolyvidone) and further comprising hydroxypropyl methylcellulose as desired.
CN101897912A Bamboo shoot sterol soft capsules and application thereof The invention discloses bamboo shoot sterol soft capsules and application thereof. The bamboo shoot sterol soft capsules comprise the following raw materials in percentage by weight: 0.01 to 20.00 percent of bamboo shoot sterol, 0.01 to 40.00 percent of vitamin E and 50.00 to 80.00 percent of vegetable oil. The bamboo shoot sterol soft capsules have the advantages of low cost, advanced and simple production process, good effect and convenient taking and carrying, are suitable for middle-aged or elderly people, and have the effect of treating prostatic disorder.
US20080241120 Therapeutic mixturecomprising pilocarpine combined with bioadhesive polymer for use in treatment of reduced salivation The object of the invention is a composition for the treatment of hypoptyalism, characterized in that it comprises pilocarpine combined with at least one bioadhesive polymer so as to allow dissolution and local attachment to the tissues of the buccopharyngeal cavity.
WO2006100527A1 Effervescent tablet containing sodium alendronate and related use and process An effervescent tablet comprising Sodium Alendronate for oral use, in treating and preventing osteoporosis in patients who have difficulty in swallowing conventional tablets.
WO2011054171A1 Tyrosine derivative histone deacetylases inhibitors and applications thereof Tyrosine derivative histone deacetylases inhibitors and preparation methods and applications thereof are disclosed. A kind of powerful histone deacetylases inhibitors, which can effectively treat the diseases of abnormal expression of the activity of the histone deacetylases, is provided. In particular, compounds having the structure of formula (I) and various optical isomers, pharmaceutically acceptable salts, solvates and prodrugs thereof are disclosed. Medicament compositions containing the compounds having the structure of formula (I) and uses of the compounds for manufacturing medicament are further provided.
WO2012113835A1 C-glucosidic ellagitannin compounds for use for altering the supramolecular arrangement of actin and for the treatment of osteoporosis, cancer, bacterial infection and viral infection The present invention concerns a C-glucosidic ellagitannin compound or a metabolite thereof for use for altering the supramolecular arrangement of actin in an individual suffering from osteoporosis, cancer, bacterial infection, or viral infection. It also pertains to pharmaceutical compositions comprising a C-glucosidic ellagitannin compound and/or metabolites thereof and one or more physiologically acceptable carriers. It finally concerns a C-glucosidic ellagitannin compound or a metabolite thereof, optionally detectably labeled, for in vitro use as a tool for studying cellular mechanisms involving actin, or for detecting F-actin in a cell.
US20050043286 Use of an ascomycin for the treatment of blepharitis This invention relates to the use of an ascomycin for the treatment of blepharitis.
CN1748700A Albendazole new form for treating nasal polyp and nasal polyp diseases The present invention relates to the preparation process of nebula, aerosol, powder spraying agent and nose drop of albendazole and their application in treating nasal polyp and nasal polyp disease and in preventing recurrence of polyp after surgical operation treatment, laser treatment and other treatment.
US20100113560 Compositions and methods for treating hematopoietic malignancies Described herein are compositions and methods for the prevention and treatment of hematopoietic malignancies. The compositions are miRNAs and associated nucleic acids.
US20120053509 Vaccines for human papilloma virus and methods for using the same Improved anti-HPV immunogens and nucleic acid molecules that encode them are disclosed. Immunogens disclosed include those having consensus HPV 6, HPV 11, HPV 33 and HPV58 E6 and E7. Pharmaceutical composition, recombinant vaccines comprising and live attenuated vaccines are disclosed as well methods of inducing an immune response in an individual against HPV are disclosed.
CN101269010B Ofloxacin injection and preparation method thereof The invention discloses an ofloxacin injection and a preparation method thereof; every 100mg of the ofloxacin injection contains 200mg of ofloxacin, 0.1 to 0.2 ml of 8 to 9 percent of lactic acid, 4 to 7g mannite, and the rest is water for injection. The preparation method is that: the mannite is added into certain quantity of water for injection to be dissolved and then is added with active carbon to be filtered, so as to form solution A; the lactic acid and the ofloxacin are slowly added into certain quantity of water for injection to be dissolved, so as to form solution B; the solution B is added into the solution A and added with the water for injection to total quantity, and the active carbon is added into the mixed solution again to be stirred and filtered, the pH value is controlled within 4.2-4.8, so as to form solution C, the qualified solution of which is carried out by secondary filter, encapsulation and sterilization to be packed into a finished product. The ofloxacin injection of the invention has stable quality and is applicable to a crowd of people, and does not contain salt and sugar, so that all the people who are sensitive strain infected persons having hypertension and diabetes mellitus can use the ofloxacin injection. The preparation method is simple and easy to be implemented, and has lower cost and good economic benefit.
EP1946762A1 Scavenger of harmful active oxygen and/or free radical in living body An object of the present invention is to provide a scavenger of in vivo harmful reactive oxygen species and/or free radicals, which is capable of effectively reducing the concentrations of in vivo reactive oxygen species and/or free radicals and exhibiting given effects such as the suppression of aging process, the prevention of geriatric or lifestyle-related disease, health promotion, and the inhibition of oxidative stress by virtue of this reduction in the concentrations of reactive oxygen species and/or free radicals. The scavenger of in vivo harmful reactive oxygen species and/or free radicals of the present invention comprises a liquid or gas comprising at least a hydrogen molecule. This medium may further comprise an oxygen molecule. Furthermore, this medium may comprise water or an aqueous solution or may be a gas. The scavenger of reactive oxygen species and/or free radicals can be used in the treatment or prevention of a disorder attributed to reactive oxygen species and/or free radicals.
US7049326 Altering a drug's distribution, metabolism and elimination properties, especially by modifying with aralkyl ester moieties to increase rate of metabolism to inactive and nontoxic metabolites when exposure is halted; surgery, riots A method for modifying at least one non-ester-containing parent compound, and the compounds produced using such method, which compounds are deployed to temporarily incapacitate at least one subject are disclosed. The modified compounds are rapidly metabolized to inactive and non-toxic metabolites when exposure to the modified compounds is halted. One or more of a predetermined chemical arrangement is incorporated into the parent compound having the formula: φ-R—X—R′; where φ is a phenyl, substituted aryl or heteroaryl system present in the parent compound or is added to the parent compound; R is an alkyl or alkene containing chain either branched or unbranched from 0 to 10 carbons present in the parent compound or is added to φ; X is a carboxyl, sulfoxyl or phosphatyl function added to R; and, R′ is an alkyl, alkenyl or aralkyl group either branched or unbranched containing from 1 to 10 carbons is added to X in a metabolically labile manner, or is a structural element already present as an inherent portion of the parent compound that is connected to X in a metabolically labile manner.
US20100004216 Medicinal lipolysis of accumulation of fat Aqueous preparations comprising at least one phospholipid or at least one bile acid and a component assisting degradation of fat such as riboflavin and water are suitable for producing medicaments for removing subcutaneous accumulations of fat and lead to regression of diet-resistant fat pads.
CN101766649A Buccal tablets for treating amygdalitis The invention relates to buccal tablets for treating amygdalitis, which comprise edible sodium chloride, edible iodine and edible glutamic acid, wherein based on the total amount of 100 percent by weight of the edible sodium chloride and the edible glutamic acid, the content of the edible sodium is not more than 0.025 percent and not less than 0.015 percent; and the ratio of the edible glutamic acid to the edible sodium chloride is that the edible glutamic acid is not more than 20 percent and not less than 15 percent and the edible sodium chloride is not more than 85 percent and not less than 80 percent. The buccal tablets provided by the invention are prepared by taking corresponding components in the given weight percent range to uniformly mix. The buccal tablets also can be uniformly mixed with a diffluent medicinal adhesive to be pressed into tablets. The medicament has simple components. The components are all common foods in daily life. The buccal tablets have no any side effects, have no rare tasting in the administering process and are suitable for the patients in different age groups to administer.
WO2007054725A3 Combination of a cdk-inhibitor and a hdac-inhibitor A first aspect of the invention relates to a combination comprising a HDAC inhibitor and a compound of formula (I) or (II), or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor. A second aspect of the invention relates to a pharmaceutical product comprising a HDAC inhibitor and a compound of formula (I) or (II), or a pharmaceutically acceptable salt thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method for treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a compound of formula (I) or (II), or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor to a subject.
CN1958060A Washing soap with effects of antiinflammation and bacteriostasis A washing soap for treating pudendal and anus itching, herpes simplex, tinea pedis, foul foot, etc, suppressing fungus, candida and crab-louse, and preventing balanoposthitis and balanus ulcer is prepared from 7 Chinese-medicinal materials including wild chrysanthemum flower, scrophularia root, dittany bark, turmeric, etc through pulverizing, mixing with glycerin, salicylic acid, and soap flake, grinding, shaping, printing and packing.
WO2012035557A1 Novel cationic amphiphiles with mannose-mimicking head-groups and a process for the preparation thereof The present invention discloses novel cationic amphiphiles containing mannose-mimicking shikimic and quinic acid head-groups and a process for preparing cationic amphiphiles with mannose-mimicking polar head-groups such as, shikimic and quinic acids. The findings described herein also demonstrate that compounds of the present invention can target model DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterpart in dendritic cell (DC, the most professional APC) based genetic immunization in mice. Cationic amphiphiles with mannose-mimicking quinic and shikic acid head-groups described in the present invention are likely to find future applications in the field of genetic immunization.
WO2006074914A2 Human rna helicase and therapeutic uses thereof The present invention provides amino acid sequences of a human RNA helicase, RHAU. The present invention specifically provides isolated peptide and nucleic acid molecules and methods of identifying modulators of RHAU peptides and nucleic acid molecules.
US7494984 Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
CN102836143A Lead-free black plaster and preparation method thereof The invention relates to a lead-free black plaster and a preparation method of the lead-free black plaster. The lead-free black plaster is prepared by vegetable oil, a therapeutic drug and a cream forming agent as raw materials. The cream forming agent is zinc oxide or ferroferric oxide. The invention has the following benefits: the lead-free black plaster is harmless to human bodies and does not pollute the environment while the lead-free black plaster is processed, and does not stimulate the skin when the lead-free black plaster is utilized; and moreover, a prepared matrix can be completely mixed with the medicinal components, the effective components of the therapeutic drug can be adjusted, and the nerve endings can be stimulated to enhance systemic circulation and accelerate the transfer and effect on promoting blood circulation of the medicines, so that the different externally-applied plasters can be prepared.
US20090285888 Derivatives of dihydroxyphenylalanine The invention relates to derivatives of dihydroxyphenylalanine, to their synthesis and to pharmaceutical compositions containing said derivatives of dihydroxyphenylalanine. Furthermore, the invention relates to the use of said derivatives of dihydroxyphenylalanine and said pharmaceutical compositions for the treatment and prophylaxis of movement disorders, neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, hemiparkinson-hemiatrophy, parkinsonian syndrome, Lewy body disease, frontotemporal dementia, Lytico-Bodig disease (parkinsonism/dementia/amyotrophic lateral sclerosis), striatonigral degeneration, Shy-Drager syndrome, sporadic olivopontocerebellar degeneration, progressive atrophy of the globus pallidus, progressive supranuclear palsy, Hallervorden-Spatz disease, Huntington's disease, X-linked dystonia-parkinsonism (Lubag), mitochondrial cytopathy with striatal necrosis, neuroacanthocytosis, restless legs syndrome, Wilson's disease.
US20130017233 Tricalcium Phosphate Coarse Particle Compositions and Methods for Making the Same Methods for preparing a tricalcium phosphate coarse particle composition are provided. Aspects of the methods include converting an initial tricalcium phosphate particulate composition to hydroxyapatite, sintering the resultant hydroxyapatite to produce a second tricalcium phosphate composition and then mechanically manipulating the second tricalcium phosphate composition to produce a tricalcium phosphate coarse particle composition. The subject methods and compositions produced thereby find use in a variety of applications.
EP1133298B1 Compositions comprising cefuroxime axetil Cefuroxime axetil in a non-gelatinous form on contact with an aqueous liquid, e.g. in the form of a solid solution in a polymer or in the form of a solid dispersion on a carrier, e.g. useful for the production of pharmaceutical compositions comprising cefuroxime axetil as an active ingredient and the use of cefuroxime axetil in the manufacture of an oral dosage form which does not exhibit an adverse food effect.
US20090041800 Methods for Treating Dependence Provided are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance with Compound A. Also provided are methods of treating at least one phase of substance dependence on at least one substance in patients and certain methods of treating at least one phase of cocaine dependence in patients.
US20120225098 Biofilm inhibiting composition Polysaccharide-containing extracts isolated from a host cell containing nucleotide sequences encoding genes pamA, pamB and pamC, wherein the extract is capable of inhibiting biofilm formation produced by gram-negative bacteria, gram-positive bacteria and fungi, and methods to inhibit biofilm formation or remove biofilms that have already formed.
CA2691736A1 Combination of 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and lopinavir for the treatment of a viral infection in a human The invention includes methods, compositions, and kits useful for treating a viral infection by coadministering 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, with lopinavir or a pharmaceutically acceptable salt thereof.
CN102627614A Diquinazoline diselenide compound as well as preparation method and bioactivity thereof The invention discloses an anti-tumor drug-diquinazoline diselenide compound as well as a preparation method and bioactivity thereof, which are the compound represented by the following general formula and the preparation method thereof. In the general formula, R1, R2, R3, R4 and R5 are as defined in the specification. The invention introduces the anti-tumor drug-diquinazoline diselenide compound prepared by the steps of with 4-chlorinated quinazoline and sodium diselenide or potassium diselenide or lithium diselenide as raw materials and water, ethanol, isopropanol, absolute ethanol, N,N-dimethyl formamide, dioxane, dimethyl sulfoxide or a mixture thereof as a solvent, reacting and synthesizing. The compounds a, h have proliferation inhibition effects on breast cancer cells MDA-MB-435 and have good anti-cancer activity.
US20100305201 Method of Treating a Tumor and Biodistribution of a Drug Delivered by Worm-Like Filomicelles Provided are filomicelle nanocarrier systems for the controlled transport and bioselective delivery of encapsulatable, cytotoxic active agents contained therein, particularly anticancer agents. Further provided are methods for controlling destabilization of the filomicelle membrane and the resulting hydrolysis-triggered, controlled release of the active agent(s) encapsulated therein by controlling the blend ratio (mol %) of hydrolysable PEO-block copolymer of the hydrophilic component(s) and of the more hydrophobic PEO-block copolymer component(s), wherein bioselective release of the encapsulated cytotoxic agents is distributed intracellularly, and wherein lowered dosage of the drug was delivered to the non-tumor organs. Thus, the filomicelle system offers enhanced tumor-selective biodistribution of a drug, and a reduced toxicity of the encapsulated drug to other organs.
CN102125591A Chrysanthemum indicum stamen itching relief liquor agent and preparation method thereof The invention relates to a chrysanthemum indicum stamen itching relief liquor agent and a preparation method thereof. The chrysanthemum indicum of a Beian village of the Hanting district of Weifang city is used for obtaining the fresh chrysanthemum indicum stamen in bud for sealing and extracting in Erguotou liquor with the alcohol concentration of 56 percent; and in the matching proportion, 1,665g of chrysanthemum indicum stamen is added to 1 litre of Erguotou liquor with the alcohol concentration of 56 percent. After the liquor is roughly filtered by 10 layers of gauze after two weeks, the chrysanthemum indicum stamen is discarded, and the slag is removed to form a liquor agent which is then stored in a sealed way. The chrysanthemum indicum stamen itching relief liquor agent disclosed by the invention is repeatedly applied in the mosquito biting position, and the itch can be relieved in 3 to 5 minutes and cannot be repeated. The invention is suitable for the rapid itching relief of any part bitten by mosquito and inhibits a brown hard lump formed after the skin of the seriously allergic people is bitten.
WO2013032087A1 Pharmaceutical composition including c3g or mulberry extracts containing c3g for preventing or treating diabetic impotence The present invention relates to a use of cyanidin-3-O-ß-d-glucopyranoside (C3G) for improving diabetic impotence. Specifically, the present invention relates to a pharmaceutical composition and to a health functional food composition including C3G for preventing or treating diabetic impotence. Further, the present invention relates to a pharmaceutical composition and to a health functional food composition including mulberry extracts containing C3G for preventing or treating diabetic impotence.
US20070105135 Charged compounds comprising a nucleic acid binding moiety and uses therefor Charged compounds are provided that comprise one or more regions of localized positive charge, compositions comprising such compounds, methods of synthesizing such compounds, methods of screening such compounds to identify those having anti-infective activity, and methods of using such compounds to prevent or inhibit infections. These compounds, and compositions containing them, have multiple applications, including use in human and animal medicine and in agriculture.
CA2054438C Additives to feminine hygiene products Nonabsorbent products and douche compositions for cleansing and placement within the vagina contain an amount of a compound effective to inhibit the production of toxic shock syndrome toxin-1 and Enterotoxins A, B and C when the products are brought into contact with the bacteria. The products and compositions of this invention are also effective in combatting streptococcal pyrogenic exotoxin and hemolysin production by Groups A, B, F and G streptococci. The compound is selected from the group consisting of monoesters of a polyhydric aliphatic alcohol and a C8-C18 fatty acid; diesters of a polyhydric aliphatic alcohol and a C8-C18 fatty acid; and mixtures thereof. The monoesters and diesters have at least one hydroxyl group associated with their aliphatic alcohol residue.
CA2800186A1 Nutritional formulations and method for treating diseases The present invention provides methods for treating retinal disorders using a nutraceutical composition comprising lutein and zeaxanthin. Methods for treating vitreomacular traction disorder and related disorders are disclosed.
EP1511487A1 Novel formulation for the parenteral application of crobenetine The invention relates to a novel formulation containing crobenetine, or one of its pharmaceutically acceptable salts, for parenteral application.
US7625890 Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
EP1899345B1 Pyrrolotriazine compounds useful as kinase inhibitors The invention relates to at least one pyrrolotriazine derivative of formula (I), at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.
US20090311329 Casein micelles for nanoencapsulation of hydrophobic compounds The present invention relates to the field of food technology and delivery of hydrophobic biologically active compounds, particularly nutrients, via food products and beverages. In particular the present invention provides isolated casein micelles useful for the encapsulation of hydrophobic nutrients, therapeutic and cosmetic compounds, compositions thereof and methods of preparing the micelles.
CA2327398C Methods and compositions for stabilizing acetylcholine compositions A pharmaceutical product which includes two-chambers, one having a buffered diluent and the other having acetylcholine. Upon mixing the chamber contents, a buffered efficacious acetylcholine product is prepared for post-surgical ophthalmic injection. Another embodiment of the invention is a method of providing an acetylcholine product which has a substantially consistent final pH without substantial degradation of the acetylcholine. The method involves storing an unbuffered acetylcholine separate from a diluent solution which has been buffered, and mixing prior to use.
US20100179138 Isozazole Compounds As Inhibitors Of Heat Shock Proteins Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —(C═S)—, —SO.sub.2-, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2—or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.
WO2014028080A1 Treatment of prostate cancer and hematologic neoplasms Prostate cancer and hematological neoplasms are treated by administration of (i) a compound of Formula I: wherein: R1 is -OH or -O-P(O)(OH)2; and R2is (II) or (III); (ii) N 6-benzyladenosine, (iii) N-(phenylmethyl)-7-β-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine, (iv) N-(phenylmethyl)-7-β-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine 5'-monophosphate; or a pharmaceutically acceptable salt thereof.
US20060052377 2-(Alpha-phenylthiobenzyl)morpholine derivatives, e.g., (4-fluorophenyl){[2-methoxyphenyl]thio}methyl)morpholine; serotonin and norepinephrine reuptake inhibitors A compound of formula (I) (I) wherein R is H; Ar is an aromatic group selected from phenyl; X is a phenyl group; R′ H or C1-C4 alkyl; each R1 is independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.
WO2013162416A1 Broncholytic drug on the basis of prostaglandin The invention relates to the field of medicine, and specifically to pulmonology, and concerns a method for treating inflammatory and obstructive diseases of the airways, in particular bronchial asthma and obstructive bronchitis, with the aid of a drug on the basis of 1',3'-dinitroglycerol ester 11(S),15(S)-dihydroxy-9-keto-5Z,13Е-prostadienoic acid (nitroproston) having a marked bronchodilatory effect. The present invention provides for an expansion of the range of broncholytic drugs by the use of a derivative of natural prostaglandin Е2, which is characterized by greater biological activity and the absence of noticeable side effects.
WO2010003232A1 Treating cancer using atractyloside The present invention provides a composition of atractyloside (ATR) or carboxyatractyloside (CATR) for treating cancer. Treatment of tumours with ATR is shown to suppress tumour growth and to enhance median survival times in a breast cancer model. ATR compositions are also shown to be useful in treating tumours refractory to other chemotherapeutic regimens.
CN101389600A Optical isomers of dihydro-2,3-benzodiazepine derivatives, process for their stereoselective synthesis The present invention relates to dihydro-2,3-benzodiazepine compounds of high enantiomeric purity according to the general formula (I), which contain an asymmetric centre at the position 4 of the dihydro-2,3-benzodiazepine compound, and the preparation thereof and the used intermediates as well. These compounds have anti-convulsive muscle relaxant and neuroprotective effect due their non-competitive AMPA antagonistic properties.
CN101073555A Injecting tanshinone II and its derivative concentrated solution and its production The invention is concerned with the injecting thick solution and the preparation method that prepares by Tanshinone IIA or Sodium Tanshinone IIA.
US6838446 Anticancer agents; genetic engineered enzyme This invention relates particularly to gene directed enzyme prodrug therapy (GDEPT) using post translational glycosylphosphatidylinositol (GPI addition to a prodrug activating enzyme to enable anchorage of the enzyme at the cell surface, particularly for use in cancer therapy. A preferred prodrug activating enzyme is carboxypeptidase G2.
US20080026020 Cosmetic composition combining a C-glycoside derivative and an associative polymer The present invention relates to a cosmetic and/or pharmaceutical composition, especially a dermatological composition, comprising, in a physiologically acceptable medium containing an aqueous medium, at least one C-glycoside derivative and at least one associative polymer.
CN103333119A 1,2-dihydro-6-methyl-4-substituted amino-5-pyrimidinecarboxylic acid compound and its preparation method and use The invention relates to a 1,2-dihydro-6-methyl-4-substituted amino-5-pyrimidinecarboxylic acid compound shown in a general formula (I) and its pharmaceutically acceptable salt or pharmaceutically acceptable solvent mixture and also relates to a preparation method thereof, a pharmaceutical composition containing the 1,2-dihydro-6-methyl-4-substituted amino-5-pyrimidinecarboxylic acid compound, and a use of the 1,2-dihydro-6-methyl-4-substituted amino-5-pyrimidinecarboxylic acid compound in preparation of drugs for prevention or treatment on diseases related to cell abnormal proliferation and morphologic change and especially for prevention or treatment on tumor growth and metastasis.
CN101306184A Common turmeric extract vein emulsion injection and its preparation method and use The invention provides Curcuma wenyujin Y.H.Chen et C.Ling extract intravenous emulsion, and a preparation method and a use thereof, in particular to novel Curcuma wenyujin Y.H.Chen et C.Ling extract injection, which relates to intravenous emulsion and a preparation method and a use thereof more specifically. The Curcuma wenyujin Y.H.Chen et C.Ling extract intravenous emulsion comprises an extract with the total content of sesquiterpene more than or equal to 70 percent by weight extracted from the volatilized Curcuma wenyujin Y.H.Chen et C.Ling through the rectification of a packed vacuum rectifier unit or a molecular distillation unit, soya lecithin, cholesterin and water for injection which are mixed uniformly. The mixture is homogenized under high pressure until dispersed phase stable aqueous dispersion with the average particle diameter less than or equal to one micrometer is got, thus preparing the Curcuma wenyujin Y.H.Chen et C. Ling extract intravenous emulsion. The drug effect of the pharmaceutical preparation is significantly improved, and the irritability of the the Curcuma wenyujin Y.H.Chen et C. Ling extract intravenous emulsion applied in intravenous injection is reduced with the improved stability.
CN102631663A Compound amino acid composition and preparation for treatment of male sterility, impotence and premature ejaculation The invention discloses a compound amino acid composition for the treatment of male sterility, impotence and premature ejaculation, which comprises arginine and proline or derivatives thereof, or pharmaceutically acceptable salts or esters, and preferably, further comprises threonine, sorbitol, magnesium sulfate and the like. According to the invention, the compositions above are preferably prepared into an external preparation, the pharmacological and toxic effects of and between the ingredients of the composition disclosed by the invention are definite, thus guaranteeing safe administration and no toxic or side effects; meanwhile, several substances with simple ingredients can also lead to excellent treatment effect, so the cost is low and the treatment expenditure of patient is lowered drastically; furthermore, the compositions are preferably prepared into an external preparation disclosed by the invention, therefore, therapeutic effect can be obtained within a short time, toxic or side effects on other organs caused by oral administration and other administration ways are avoided simultaneously, the amount of medicines is also greatly reduced, and safety in administration in improved while treatment expenditure is lowered, so significant economic and social benefits are contained in the compound amino acid composition.
WO2013029297A1 Use of patchouli alcohol in preparation of drug against helicobacter pylori The present invention relates to a use of patchouli alcohol in the preparation of a drug against Helicobacter pylori. The drug according to the present invention is composed of the patchouli alcohol and pharmaceutically acceptable additives, wherein the content of the patchouli alcohol is 0.5-70%. The patchouli alcohol according to the present invention has a quite narrow antimicrobial spectrum, and may selectively inhibit Helicobacter pylori without influencing growth and propagation of other bacterial populations (including other gram negative bacteria). The patchouli alcohol may kill Helicobacter pylori without damaging probiotics, and may keep an ecological balance of bacterial populations in the intestinal tract of human body. Therefore, the patchouli alcohol may be used for treatment of diseases caused by infection of Helicobacter pylori, such as gastritis, peptic ulcer and early gastric cancer.
CN1838958A Methods of treating COPD and pulmonary hypertension Disclosed are methods of treating COPD and Pulmonary Hypertension using p38 Map Kinase inhibitors in combination with one or more other active ingredients.
US20080194608 Atherosclerosis therapy; antidiabetic agents; dyslipidemia Compounds of the formula (I): in which R1, R2, R3, R′3 and R4 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, the pharmaceutical compositions comprising them, and the processes for the preparation of these compounds.
CN102824452A Pain relieving fitness paste and production method thereof The invention relates to a pain relieving fitness paste and a production method thereof which are mainly used for providing medication for treating the pain caused by osteomyelitis, arthritis and hyperosteogeny. The pain relieving fitness paste is prepared from 90-120g of radix salviae miltiorrhizae, 90-120g of safflower, 90-120g of caulis spatholobi, 90-120g of fructus gardeniae, 45-65g of radix clematidis, 45-65g of radix angelicae pubescentis, 45-65g of pricklyash peel, 130-165g of borneol, 90-120g of camphora and 90-120g of menthol crystal. The production method comprises the following steps of: grinding the radix salviae miltiorrhizae, safflower, caulis spatholobi, fructus gardeniae, radix clematidis, radix angelicae pubescentis and pricklyash peel into coarse powder; percolating the coarse powder with ethanol; concentrating the percolate into extract; extracting the dregs with gasoline to obtain extraction oil; preparing rubber paste, rosin, zinc oxide, wool fat, yellow vaseline, liquid paraffin, gasoline or SIS, liquid paraffin, glycerol ester of rosin and 2,6-butylated hydroxytoluene into a matrix; adding the extract, extraction oil, borneol, camphora and menthol crystal; and smearing the obtained product on the base cloth, covering with an anti-sticking layer, and slicing. Through the invention, the formula is scientific and reasonable, the active ingredients are maintained to the greatest degree, and the curative effect is improved.
WO2010122575A3 Process for the preparation of pure paliperidone The present invention provides pure Paliperidone comprising less than about 0.1%, preferably less than about 0.05% of PLP keto impurity as well as purification processes for preparing thereof.
CN101717425A 11,23,24-Tris-oxygen-butyryl alisol A ,as well as medicine composite and application thereof The invention provides a 11,23,24-Tris-oxygen-butyryl alisol A compound which is shown as formula (I), a medicine composite containing the 11,23,24-Tris-oxygen-butyryl alisol A compound shown as the formula (I), as well as officinal carrier and/or excipient, a preparation method of the compound shown as the formula (I), and an application of the compound shown as the formula (I) in medicines, in particular to medicines for inhibiting anti-hepatitis B and treating hepatitis B.
CN102875575A Cefodizime sodium compound and preparation thereof The invention relates to cefodizime sodium, in particular to a compound of the cefodizime sodium and a preparation of the compound. The compound of the cefodizime sodium is crystal, an X-ray powder diffraction diagram obtained by Cu-K alpha ray measurement is shown as a diagram 1, the grain diameter of the compound cefodizime sodium ranges from 70 micrometers to 120 micrometers, distribution width ranges from 50 micrometers to 150 micrometers, preferably, the grain diameter of the compound ranges from 80 micrometers to100 micrometers, and the distribution width ranges from 60 micrometers to140 micrometers. The crystal compound of the cefodizime sodium is good in stability and applicable to being prepared into power injection for clinical applications.
CN103508952A Salts of N-nornuciferine derivatives The invention relates to fumarates of N-nornuciferine and N-nornuciferine derivatives or pharmaceutically acceptable solvates thereof, and an application of the fumarates and the solvates in preparation of acetylcholinesterase inhibitor drugs.
EP2203438A1 Cyanoisoquinoline This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides a process for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).
CN101103963A Levalbuterol hydrochloride orally disintegrating tablet and preparation method thereof The invention relates to a levalbuterol hydrochloride orally disintegrating tablet and the preparation method; wherein the levalbuterol hydrochloride orally disintegrating tablet comprises an active pharmaceutical ingredient, the levalbuterol hydrochloride, and pharmaceutical necessities. The pharmaceutical necessities include a disintegrant, a filling agent, a masking agent and a corrective. The raw material ingredients calculated by weight ratio are 0.79-2.5 per cent levalbuterol hydrochloride, 50-60 percent disintegrant, 20-40 per cent filling agent, 1.58-10 per cent masking agent and 10-12 per cent corrective, which are made into the orally disintegrating tablets by direct powder compression process. The tablets of the invention is taken easily without water, disintegrated quickly and takes effect quickly, high in bioavailability, less stimulatory function to gastrointestinal tract, and applicable to prevention and cure of bronchial asthma, asthmatic bronchitis, and bronchospasm of an emphysema patient.
US20080227809 hexaquis(3-phenyl-propylamine) decavanadate (V); particularly insulin-resistant diabetes; insulin mimickers This invention provides compounds and pharmaceutical compositions thereof for treating human type 1 and type 2 diabetes, particularly insulin-resistant diabetes.
WO2009034390A1 Heterocyclic derivatives and their use in treating hepatitis c Use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or alleviating HCV, formula (I): wherein R1, R2, R4, Y1, Y2, Y3, A, B and W are as defined in the specification.
EP1687337A1 A method for the treatment of malignant diseases by inhibiting nucleolin Use for anti-nucleolin angents, such as antibodies, antisense molecules and interfering RNA molucules, in the treatment of cancers. The treatment is preferably combined with the administration of a chemotoxic or chemotherapeutic agent, or with radiation therapy.
CN101066251A Dispersed tablet of proton pump inhibitor The dispersed tablet of proton pump inhibitor is used for treating gastric ulcer, duodenal ulcer, stomal ulcer and other indications. It contains at least one kind of proton pump inhibitor and at least one kind of biologically acceptable buffering agent in the weight ratio of 1 to 10-200. The proton pump inhibitor is one selected from omeprazole, S-omeprazole, pantoprazole, lansoprazole, rabeprazole, leminoprazole, tenatoprazole and their salts. The biologically acceptable buffering agent is sodium bicarbonate, sodium carbonate, magnesium carbonate, etc or their mixture.
EP1494669A1 Medicament for preventing and/or treating chronic rejection This invention relates to a new use of a compound of the following formula (I) or (II) for the manufacture of a medicament for preventing and/or treating chronic rejection in a transplanted organ or tissue.
US20100266618 Compositions and methods for augmenting activity of oncolytic viruses Disclosed are compositions and methods for augmenting activity of oncolytic viruses. Virus activity is augmented by sensitizing cancer or tumour cells through modulation of the Endoplasmic Reticulum (ER) stress response pathway, for instance by introducing into a tumour cell an agent effective to modulate ER stress response and sensitize the tumour cell. The tumour cells are then contacted with an oncolytic virus in an amount effective to reduce viability of the sensitized tumour cell. The oncolytic virus is thereby rendered more effective at lysing or killing the sensitized tumour or cancer cells.
WO2006030977A3 Imidazole derivatives as large conductance calcium-activated k channel openers An imidazole compound of the formula (1): wherein Ring A is benzene or a heterocyclic ring; G is alkylthio, alkylsulfonyl, optionally substituted phenyl, or optionally substituted heterocyclic ring group, etc.; Ring C is imidazole; R1 is carbamoyl, etc.; R2 is cyano, nitro, hydroxyl, an alkoxy, a halogen, carboxy, an alkoxycarbonyl, carbamoyl, amino, an alkyl, etc.; m is 0 to 2; and R4 is hydrogen, an alkyl, etc., or a pharmaceutically acceptable salt thereof, is a large conductance calcium-activated K channel opener useful for treatment of pollakiuria, urinary incontinence, etc.
CN103251552A Enrofloxacin cataplasm and preparation method thereof The invention provides an enrofloxacin cataplasm which is prepared from raw material medicines and auxiliary materials in parts by weight: 2.5-7.5 parts of enrofloxacin, 1-3 parts of ethylparaben, 15-20 parts of glycerol, 60-100 parts of powdered sugar, 30-70 parts of liquid paraffin, 100-130 parts of wool fat, 180-200 parts of vaseline and 0-40 parts of octadecanol. The invention further provides a preparation method and use of the enrofloxacin cataplasm. The cataplasm is adopted to be attached to the palate of a piglet, the piglet can swallow automatically and the cataplasm is not easy to spit out, so that the piglet is prevented from being irritated, the growth of the piglet is not affected, and the cataplasm is convenient to feed. The cataplasm is stable in quality, and the maintaining time of blood concentration in vivo is longer. The cataplasm is slowly eliminated and the effect is prolonged, and the plasma medicine peak concentration is relatively slow to the benefit of reducing the toxic and side effects, so that the cataplasm is safer and more reliable to use.
EP2589385A1 Triple combination for the treatment of cancer The present invention relates to a triple combination comprising a nodal/activin pathway inhibitor, a hedgehog pathway inhibitor and a chemotherapeutic agent and its use as a medicament for the treatment of cancer.
CN103536577A Tenofovir dipivoxil fumarate capsule and preparation method thereof The invention relates to the field of medicines, and particularly relates to a tenofovir dipivoxil fumarate capsule and a preparation method thereof. The capsule disclosed by the invention is prepared from the following components in parts by mass: 300 parts of tenofovir dipivoxil fumarate, 40-60 parts of milk sugar, 10-40 parts of microcrystalline cellulose, 0.5-2 parts of superfine silica powder and 2-5 parts of magnesium stearate, which are filled into 1000 empty capsules.
US20090239937 Apoptosis-Inducing Genes for Treating Cancer The invention provides materials and methods related to the use of recombinant nucleic acid molecules containing an expression control element of an inhibitor of apoptosis protein (IAP) gene operatively linked to a coding region for an active cytotoxic/cytolytic agent. The recombinant molecules are used in methods to treat a variety of diseases and disorders, including a wide range of cancers.
WO2010135976A1 1-(substituted benzyl)-5-trifluoromethyl-2-(1h) pyridone compounds and their salts, their preparation methods and use thereof 1-(Substituted benzyl)-5-trifluoromethyl-2-(1H) pyridone compounds and their pharmaceutical acceptable salts are disclosed. The preparation methods of the compounds and their salts and the use of the same for preparing the medicaments for treating fibrosis are also disclosed. New pyridone compounds and their salts are obtained from trifluoromethyl pyridone as starting material.
US6939866 Antitumor agents; skin disorders; anticancer agents The invention concerns quinazoline derivatives of Formula (I) wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description; process for the preparation, pharmaceutical compositions them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
CA2651405A1 36 -des (3 -methoxy-4 -hydroxycyclohexyl) 36 - (3 -hydroxycycloheptyl) derivatives of rapamycin for the treatment of cancer and other disorders The present invention relates to novel 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives in the treatment of cancer and / or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft: vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.
US20100041768 Composition and method of adipose cell differentiation inhibition The present invention is related to a composition and method of adipose cell differentiation inhibition.
CN101361922A External drug for treating rheumatoid The invention relates to the ingredients of an external-used medicine which is used for treating rheumatoid diseases and a preparation method thereof. The purpose of the invention is to provide the external-used medicine which is used for treating rheumatoid diseases and can improve the microcirculation and relieve the symptoms of the diseases by eliminating dampness after the medicine is applied externally and absorbed by the skin and the arthrosis. The external-used medicine used for treating rheumatoid diseases comprises the following ingredients: 6 grams of Araceae, Divaricate Saposhnikovia Root, Angelica dahurica Benth. et Hook, Rhizoma Gastrodiae, Notopterygium root and Rhizoma typhonii respectively which are cut into segments, 30g of slightly baked isinglass, 30g of baked-to-yellow West Lake lotus root powder, 30g of stir-baked copperas, 9g of vermilion, 5g of Xuchangqing, 5g of Balloon Flower, 10g of Caulis Lonicerae, 5g of Forsythia, 5g of Indian Dendranthema Flower, 10g of Trichosanthes Root, 5g of Calamus and 10g of Spina Gleditsiae. The medicine is ground into fine powder, and blended with hot liquor. After the ingredients are adopted, in treating the rheumatoid diseases caused by noxious dampness such as weak renal Qi, spasm of muscles, weak contraction bi, the medicine can realize addressing both the symptoms and root causes by integrating the effect of each raw material.
US20120316127 Method of manufacturing coating agent for drug releasing stent and coating agent for drug releasing stent manufactured thereby This invention relates to a method of manufacturing a coating agent for a drug releasing stent and to a coating agent for a drug releasing stent manufactured thereby. This method includes (1) dissolving polyurethane in tetrahydrofuran, (2) dissolving pluronic F-127 in tetrahydrofuran, (3) dissolving a gemcitabine compound in ethanol, (4) mixing these three solutions obtained in (1) to (3) thus preparing a solution mixture, (5) applying the solution mixture obtained in (4) on a stent coated with a Teflon film, (6) drying the stent of (5) for a predetermined period of time and then immersing the stent in a polyurethane solution in tetrahydrofuran, and (7) removing the stent immersed in (6) from the polyurethane solution and then drying the stent, so that the rate of release of an anti-cancer drug applied on the stent can be continuously and maximally improved thereby maximizing anti-cancer efficacy.
WO2006116591A3 Ophthalmic formulations comprising prednisolone acetate and tobramycin and uses thereof Provided by the present invention are compositions or formulations suitable for application to a patient's eyes which utilizes a topical ophthalmically-acceptable formulation comprising a therapeutically-effective amount of an ophthalmically-active antimicrobial agent, and an ophthalmically-active anti-inflammatory or steroidal agent in combination with physiologic levels of serum electrolytes in an ophthalmic formulation for the treatment of changes in the normal eye condition. The invention also includes methods of treating patient's having an ophthalmic disease, injury or disorder, utilizing the compositions or formulations. Also provided are kits comprising the compositions or formulations and a means of applying the compositions or formulation to the patient's eyes.
WO2008139314A1 Compositions and methods for treating joint disorders Methods and compositions for the treatment of joint disorder in a patient, particularly a human patient, are disclosed. In particular, compositions are disclosed that contain a proteolytic enzyme inhibitor, preferably proanthocyanidins, lysine and one or more of proline, hydroxyproline, collagen and collagen derivatives. The compositions are useful for treating a joint disorder, such as joint inflammation or arthritis, including osteoarthritis and rheumatoid arthritis.
US20090012033 Delivery of Biologically Active Materials Using Core-Shell Tecto(Dendritic Polymers) The present invention concerns core-shell tecto (dendritic polymers) that are associated with biologically active materials (such as nucleic acids for use for RNAi and in transfection). Also included are formulations for their use. The constructs are useful for the delivery of drugs to an animal or plant and may be in vivo, in vitro or ex vivo.
CN103212086A Podophyllotoxin nano prodrug with high drug loading capacity and preparation method and application thereof The invention discloses a prodrug of a podophyllotoxin (POD) derivative. The prodrug is formed by acid-sensitive imine bond covalent combination of a medicine molecule and hydrophilic short-chain polyethylene glycol (PEG), wherein the medicine molecule is the podophyllotoxin derivative namely amino podophyllotoxin (NPOD), and the drug loading capacity can reach over 35%. The prodrug can form a micelle with a nano structure through a self-assembly manner in a water solution. The invention further discloses application of a self-assembled prodrug micelle as a novel medicine carrier to loading hydrophobic drugs such as taxol to realize the co-therapeutic effect of the medicine. The prodrug disclosed by the invention has the advantages of simple preparation method, environmental friendliness and economical benefit, and has greater application value in the biomedical field.
CN103432093A Pridinol methanesulfonate matrix sustained-release tablet and preparation method thereof The invention discloses a pridinol methanesulfonate matrix sustained-release tablet which is composed of the following components in percentage by mass: 6% of pridinol methanesulfonate, 20-30% of hydroxypropyl methylcellulose K4M, 10-30% of ethyl cellulose, 35-50% of starch, 1-2% of sodium carboxymethyl cellulose and 0.5-3% of magnesium stearate. After being orally taken, the sustained-release tablet is subjected to aquation to generate gel when meeting digestive juice, and the medicines are released in a dispersion or gel matrix corrosion mode. The sustained-release tablet has the advantages of advanced prescription, stable product quality, sustained medicine release, enduring drug effect and smooth blood concentration; and the wet-process granulating preparation method has the advantages of simple production technique, low cost and controllable preparation quality, and is suitable for industrialized large-scale production.
CN102018703B Azulene sulfonate-containing gynaecological special lotion The invention discloses azulene-sulfonate-containing gynaecological special lotion. The gynaecological special lotion is prepared from azulene sulfonate and metronidazole, wherein every 500 millimetres of lotion comprises 0.05 to 2.5 grams of azulene sulfonate, 1 to 3 grams of metronidazole and the balance of pure water, and further comprises golden cypress, radix sophorae flavescentis, common cnidium fruit and rhizoma atractylodis, wherein every 500 millimetres of lotion comprises 0.05 to 2.5 grams of azulene sulfonate, 1 to 3 grams of metronidazole, 5 to 10 grams of golden cypress, 5 to 10 grams of radix sophorae flavescentis, 10 to 25 grams of common cnidium fruit, 5 to 10 grams of rhizoma atractylodis and the balance of pure water. The azulene sulfonate-containing gynaecological special lotion is easy to prepare and convenient to use, has good effects of diminishing inflammation and relieving itching, can resist bacteria strikingly without side effects, and cannot stimulate mucousmembranes and skins. Furthermore, the lotion can relieve and eliminate various unwell symptoms of women caused by episioitis and vaginitis, and also can improve the self disease resistance of a female reproductive system.
CN102010423A Crystal form II of (S)-alpha, alpha-[(2-chlorphenyl)-(4,5,6,7-tetrahydrothieno [3,2-c] pyridine-5-yl)]-N'-(dimethyl) methylene) acethydrazide and preparation method The invention relates to a crystal form II of (S)-alpha, alpha-[(2-chlorphenyl)-(4,5,6,7-tetrahydrothieno [3,2-c] pyridine-5-yl)]-N'-(dimethyl) methylene) acethydrazide and a preparation method, and also relates to a medicinal composition prepared by the new crystal form II and application. The crystal form II is characterized by a powder X-ray diffraction pattern and melting point data of the crystal form II.
WO2011121055A1 Pyridinyl derivatives comprising a cyanoguanidine or squaric acid moiety The present application discloses compounds of the formula (I) wherein X = opt.subst. pyrid-3-yl or pyrid-4-yl; Q = opt.subst. Ci-6 alkylene or a single bond; Y is formula (i) wherein D is = N-CN, or formula (ii) B = is opt.subst. C1-6 alkylene; A = (formula) Z = -J-V, wherein J = -C(=0)-, -C(=O)-O, -S(=O)2-, -P(=O)(OR4)-, -C(=O)-NR4- and -C(=S)-NR4-, and V = opt.subst. C1-12-alkyl, opt.subst. C3-12-cycloalkyl, -[CH2CH2O]1-10-( opt.subst. C1-6-alkyl), opt.subst. C1-12- alkenyl, opt.subst. aryl, opt.subst. heterocyclyl, or opt.subst. heteroaryl; q = 0-2, and r = 0- 2; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
CN102048160A Use of ampelopsin in preparation of healthcare food and medicaments for protecting vascular endothelial cells The invention discloses the use of ampelopsin in the preparation of healthcare food and medicaments for protecting vascular endothelial cells. In the invention, purified ampelopsin or unpurified ampelopsin-containing extract is prepared into pharmaceutically allowable preparations for oral taking, injection or external application. The ampelopsin protects the vascular endothelial cells by reducing peroxidation of lipid, resisting oxidative damage and other actions, so as to prevent and treat cardiovascular and cerebrovascular diseases caused by endothelial cell injury, such as atherosclerosis, hypertension and cardiac-cerebral thrombosis.
EP1711161A2 Methods of preventing and treating sars using low ph respiratory tract compositions The present invention is directed to methods of preventing and treating Severe Acute Respiratory Syndrome (SARS) by the administration of respiratory tract compositions having low pH values. The respiratory tract compositions have a pH of from about 3.0 to about 5.5, and are preferably administered to areas of the respiratory tract such as the nasal cavity to effectively prevent and treat respiratory tract viral infections, particularly SARS. The respiratory tract compositions comprise an organic acid in combination with a metal compound.
EP1608351B1 Compositions containing superoxide dismutase and a selected et 5-lipoxygenase inhibitor and uses thereof The invention relates to compositions containing at least one superoxide dismutase (SOD) and at least one appropriately selected 5 lipoxygenase (5-LO) inhibitor, and to the uses thereof as medicaments or dietary products for the prevention and/or treatment of allergy-based or non-allergy-based chronic inflammatory diseases.
CN101328156A Hydroxamic acids derivates containing 1,3 biheterocycle five-membered rings and use thereof The invention relates to the medicine field related to the infection, in particular to a hydroxamic acid derivative containing 1, 3 two hetero five-membered ring, a salt acceptable in pharmacology and a preparation method thereof as well as a medicine composition containing the hydroxamic acid derivative and the salt. The hydroxamic acid derivative has a structure shown in formula I. The derivative and the composition thereof have the antibiosis function, wherein the definition of each group is stated in the instruction.
US20090137557 Calcilytic Compounds Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.
CN1679611A Compound preparation of piracetam and its use A high-energy composite medicine for treating acute or chronic cerebrovascular disease, cerebral trauma, toxipathic cerebrosis, hypomneis and cerebral disfunction contains proportionally inosine, ATP, VC and piracetam.
CA2302228C Sterilized 5-aminolevulinic acid Colored 5-aminolevulinic acid crystals useful for photodynamic therapy are disclosed. Preferably the colored 5-aminolevulinic acid crystals have the color imparted by irradiation of the crystals, such as gamma radiation. The colored ALA crystals are preferably pharmaceutically pure and sterile and can be contained in a sealed sterile container. Also disclosed is sterile aqueous ALA solution which includes the colored ALA crystals contained in water. Also disclosed is a method for preparing colored ALA crystals which includes exposing non-irradiated ALA crystals to a radiation source at a dose sufficient to impart a color which is different than any color present in the non-irradiated crystals. Preferably the irradiation is sufficient to sterilize the ALA crystals. The sterile colored ALA crystals can be used in a kit for internal or external treatment and/or detection of a condition in a mammal, which includes the sterile, colored ALA crystals and sterile diluent, and in the case of internal treatment and/or detection optionally a catheter for administration of the ALA.
US7585884 Pleconaril; reduced side effects Oxadiazolyl-phenoxyalkylisoxazoles and pharmaceutically acceptable salts thereof, compositions comprising oxadiazolyl-phenoxyalkylisoxazole compounds or pharmaceutically acceptable salts thereof and methods for using oxadiazolyl-phenoxyalkylisoxzazole compounds or pharmaceutically acceptable salts thereof as anti-picornaviral agents are described herein. The methods include using pleconaril as a prodrug for conversion to anti-picornaviral compounds in vivo.
US20080085876 Insect sting treatment A treatment for insect bites and stings [100] includes a mixture of a base material [101], a draw-out agent [102], an immune suppression agent [103] for reducing an immune response, and optionally, an antimicrobial agent [104]. The draw-out agent [102] functions to keep the wound moist and open. The immune suppression agent [103] reduces the body's immune reaction keeping the wound open allowing for ejection of foreign bodies, microbes and toxins. The natural antimicrobial properties of the antimicrobial agent [104] kill the microbes. Optionally, the treatment [100] may include insect venom antidotes [105] to neutralize the venom's effect.
WO2013037862A1 Specific phosphatidylcholines as modulators of platelet activation factor activity The present invention relates to a pharmaceutical composition or a medicament for use in preventing or treating a PAF-related disease, comprising a phosphatidylcholine of formula (I), and also to the use of such a compound as a medicament or as a modulator of PAF activity.
US20110014202 Methods for Diagnosing and Treating Neuroendocrine Cancer The present invention relates to a method for diagnosing neuroendocrine cancers via detecting the presence of N-methyl D-asparate-associated (NMDA) glutamate receptors type 1 and/or type 2. Methods for preventing and treating neuroendocrine cancers are also disclosed.
US7396823 Therapy inhalation involving antisense oligonucleotides for treating idiopathic pulmonary fibrosis The invention provides antisense DNA oligonucleotides which are effective in inhibiting the expression of a wild type COL1A1 gene, wherein said oligonucleotides are used in inhalation therapy to treat various lung diseases.
WO2012059594A1 Mineralcorticoid receptor antagonists for the treatment of corticoid-induced obesity The present invention is on the field of prevention and/or treatment of adipogenesis and obesity. According to the invention mineralcorticoid receptor antagonists are used as the therapeutically active principle. The mineralcorticoid receptor antagonists used in this invention are capable of displacing the endogenous glucocorticoid cortisol from the antimineralcorticoid receptor.
US7449475 e.g. 2-{[(2S)-3-(5-Chloro-1'H,3H-spiro[1-benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-N-cyclopropylbenzamide; macrophage inflammatory protein (MIP)-1 alpha chemokine receptor modulator; antiinflammatory, antiproliferative agent, autoimmune diseases The invention provides compounds of formula (I) wherein m R1, n, R2, q, X, Y, Z, R3, R4, R5, R6, R7, R8, t, and R9 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
EP2147918A1 Process for the preparation of S-omeprazole magnesium in a stable form There is provided a process for preparing purified esomeprazole magnesium, comprising the steps of: providing esomeprazole magnesium; contacting said esomeprazole magnesium with a non-solvent comprising an aqueous component up to a maximum content defined by water saturation in the non-solvent; and recovering purified esomeprazole magnesium formed from the contacting step. The process is particularly suitable to obtain esomeprazole magnesium dihydrate, expecially form A. The esomeprazole magnesium obtained is remarkably pure, stable and is resistant to form interchangeability.
US7074794 pyrrolo-2yl-carbonyl-amino compounds; dipeptidyl peptidase inhibitor The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
US7091230 2-aryloxy-2-arylalkanoic acids for diabetes and lipid disorders A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
US7022704 5,6,7, 8-tetrahydro-imidazo-(1,2a)-pyrazine derivative; useful for treating restenosis and tumor A family of tetrahydroimidazo[1,2a]pyrazine based compounds capable of inhibiting the activity of farnesyl transferase and treating tumors and restenosis having the following structure: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined in the specification.
CN103520302A Sea-buckthorn leaf anti-fatigue capsule and preparation method thereof The invention relates to a health care medicine, specifically to an anti-fatigue capsule with a sea-buckthorn leaf or an extract thereof as a main raw material and a preparation method thereof. To overcome a technical problem, the invention provides an anti-fatigue health-care capsule with the sea-buckthorn leaf as a main raw material and a preparation method thereof. According to a technical scheme provided by the invention, the sea-buckthorn leaf anti-fatigue capsule comprises the following raw materials by mass: 500 to 550 parts of the sea-buckthorn leaf, 180 to 200 parts of rhodiola root, 100 to 150 parts of prepared fleece flower root, 80 to 100 parts of dogwood, 60 to 80 parts of milkvetch root, 40 to 60 parts of eucommia bark, 50 to 60 parts of epimedium, 40 to 60 parts of tree peony bark, 30 to 40 parts of ginseng and 20 to 30 parts of calcium gluconate. The above-mentioned raw materials undergo crushing, extraction, freeze drying, mixing, granulation, drying, sterilization and capsule filling so as to prepare a finished anti-fatigue capsule product.
US6953778 Methods and compositions for the diagnosis and treatment of hematological disorders using 2777 The present invention relates to methods and compositions for the diagnosis and treatment of hematological disorders, including, but not limited to, apalstic anemia, hemophilia, sickle cell anemia, thalassisemia, blood loss and other blood disorders, e.g., blood diorders related to bone marrow irradiation or chemotherapy treatment or renal failure. The invention further provides methods for identifying a compound capable of treating a hematological disorder. The invention also provides methods for identifying a compound capable of modulating a hematopoietic cell activity. Yet further, the invention provides a method for modulating a hematopoietic cell activity. In addition, the invention provides a method for treating a subject having a hematological disorder characterized by aberrant 2777 polypeptide activity or aberrant 2777 nucleic acid expression. In another aspect, the invention provides methods for increasing hematopoietic cell proliferation in a subject and methods for modulating hematopoietic cell apoptosis in a subject.
WO2010119347A1 Netupitant for use in treating bladder dysfunction The present invention relates to methods for reducing the frequency of bladder contractions without significantly affecting micturition pressure, comprising administering a pharmaceutical composition comprising a therapeutically effective amount of netupitant, or a pharmaceutically acceptable salt or prodrug thereof. The method can be used to treat bladder dysfunction without significantly increasing residual volume, including urgency, frequency, pollakiuria, nocturia, low deferment time, suboptimal volume threshold, neurogenic bladder, or combinations thereof.
US7326785 Preparation of 3-(thienylalkenylenesulfonylamino)-1-(4--morpholinylcarbonyl-alpha-substituted methyl)pyrrolidone derivatives: 2-(5-Chlorothien-2-yl)-N-methyl-N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}ethenesulfonamide The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
CN102617546A Aromatic iodonium salts as NADH oxidase inhibitors and anti-tumor application thereof The invention provides a series of novel aromatic iodonium salt compounds that are used as NADH (reduced form of nicotinamide-adenine dinucleotide) oxidase inhibitors, and discovers the new anti-cancer application of the novel aromatic iodonium salt compounds and a few of other known NADH oxidase inhibitors. The iodonium salts can inhibit the activity of NADH oxidases in in-vitro assays, and can obviously inhibit the growth of malignant cells of humanized pancreatic cancer, multiple myeloma, esophageal carcinoma, intestinal cancer and the like. To aim at new anti-cancer targets, the development of novel anti-tumor drugs can be carried forward.
US20110190328 Acid addition salts of (3,5-bis trifluoromethyl)-n-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide The present invention relates to acid addition salts of the pharmaceutically active compound (3,5-Bistrifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide(I): The invention also relates to processes for the preparation these acid addition salts and to their use as anti tumor agent in humans.
WO2005096717A2 Agent exhibiting hepatoprotective properties The invention relates to medicine, in particular a hepatoprotective and anti-encephalopathic agent for reducing alcohol intoxication. Said invention is characterised in that, apart from components based on amber, boletic and glutaminic acids, said agent contains at least one type of a group B vitamin. The inventive agent can also contain vegetable extracts or the mixtures thereof, L-carnitine, glicine, L-arginine, taurin and/or the mixture thereof, methyl-sulphonyl-methan, dihydroquercinite, dimethylsulphoxide or the mixture thereof, nicotinamide or nicotinic acid or the mixture thereof, energiser and a sweetener. A method for reducing alcohol intoxication, preventing and removing alcohol withdrawal syndrome, protecting a liver including encelopathy protection at non-alcohol intoxication is also disclosed. The invention enables to use said effects without qualified medical monitoring.
US7361681 Method of treating amytrophic lateral sclerosis using melatonin The present invention relates to the treatment of amyotrophic lateral sclerosis (ALS) and/or the improvement of motor function in individuals in need of such improvement using a melatonin compound or a pharmaceutical salt of the melatonin compound.
US20080131519 Omega-3-polyunsaturated fatty acid ester, in fish oil concentrate containing a 5,8,11,14,17-eicosapentaenic acid ester and a 4,7,10,13,16,19-docosahexaenic acid ester, also lysine of a salt, optionally a zinc salt, or selenium The invention relates to a novel antiviral and immune-simulating pharmaceutical composition, containing as active ingredient 20-85 mass % of a ω-3-polyunsaturated fatty acid ester, in fish oil concentrate containing 20-70 mass % of a 5,8,11,14,17-eicosapentaenic acid ester and a 4,7,10,13,16,19-docosahexaenic acid ester, further 1-lysine of a salt thereof, optionally a zinc salt, selenium or a selenium compound, as well as additives and carrier ingredients.
CN102085199A Percutaneous absorption biological patch for treating rheumatoid arthritis and preparing method thereof The invention relates to a percutaneous absorption biological patch for treating rheumatoid arthritis and preparing method thereof. The biological patch consists of basic remedy treating for the rheumatoid arthritis, medicament solvent, adhesive, biological plaster matrix and percutaneous absorption penetration enhancer. The basic remedies treating for the rheumatoid arthritis include triptolide and analgesics lidocaine hydrochloride alleviating the pain of the rheumatoid arthritis. The biological plaster has comprehensive pharmacological effect, exactly blocks up the main pathology link of development of rheumatoid arthritis, has strong pertinency and lasting pharmacological effect; and can be prepared by using a general method in biological plaster preparing technology field; and the preparing method is simple.
CN101766585A Medical paste film The invention belongs to the field of external application of skin and skin medicine. The basic recipe of the medical paste film comprises polyvinyl alcohol, sodium carboxymethyl cellulose, and gelatinase dialyzed and purified product. The medical paste film is characterized in that after the product is applied on the skin or wound, a layer of ultrathin microporous air-permeable film closed to the skin can be formed, so as to resist external dust and bacteria, and can provide medicine and nutrients for the interior. By adding different medicines into the basic recipe, products with different efficacies can be obtained. The medical paste film can be used for curing diseases such as skin disease, muscle disease and neuralgia, can promote wound healing and facilitate observation and treatment when being applied in the operation stitching position, can overcome the disadvantage that the skin medicine is easy to rub off, can not lead to skin allergy, and can be washed with water when not in use.
EP1889845A1 Novel pleuromutilin derivatives Pleuromutilin compounds of the formula (A) & (B) are of use in anti-bacterial therapy. in which: R1 is optionally substituted C(1-6)alkyl or C(3-6)cycloalkyl or optionally substituted heterocyclyl; R2 is vinyl or ethyl; R3 is H, OH or F, and R4 is H, or R3 is H and R4 is F, and R5 and R6 together form an oxo group; or R3 and R4 is each H, R5 is OH or H and R6 is H, or R5 is H and R6 is OH or H.
US20110196021 High Affinity Nucleic Acid Ligands of Complement System Proteins Methods are described for the identification and preparation of high-affinity Nucleic Acid Ligands to Complement System Proteins. Methods are described for the identification and preparation of high affinity Nucleic Acid Ligands to Complement System Proteins C1q, C3 and C5. Included in the invention are specific RNA ligands to C1q, C3 and C5 identified by the SELEX method.
CN101810597A Transdermal patch containing vauqueline and preparation method and application thereof The invention discloses transdermal patch containing vauqueline and a preparation method and an application thereof. The transdermal patch consists of a back sheet, a protective layer and a medicine-containing matrix layer, wherein the medicine-containing matrix layer consists of vauqueline, hydrophilie matrix and penetrating agent, wherein the penetrating agent is selected from one or more of azone, oleic acid, propanediol and menthol. The vauqueline patch has scientific and reasonable proportion. Particularly the hydrophilie matrix is adopted, so the loaded dosage can be increased, and the vauqueline is effectively promoted to be released through the adhesive layer so as to improve the bioavailability. Moreover, the vauqueline patch is proved in the Pharmacodynamics experiment that stable blood medicine concentration can be maintained after the percutaneous absorption of the vauqueline patch, good pain-killing and anti-inflammatory effect can be played when the toxicity thereof is prevented, the preparation process has strong maneuverability, and the industrialized production can be realized.
EP1874776A1 Oxazole and thiazole compounds and their use in the treatment of pge2 mediated disorders Compounds of formula (I) or a pharmaceutiically acceptable derivative thereof: wherein X, Z, Y', Y'', R1 ,R2a, R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
CN103211837A Application of arsenic trioxide in preparation of medicines for treating renal carcinoma The invention discloses application of arsenic trioxide in preparation of medicines for treating renal carcinoma. The key point of the technical scheme is that arsenic trioxide inhibits proliferation of human renal carcinoma cells 786-O by inhibiting the PI3K-Akt transduction path, so that arsenic trioxide can be used for preparing medicines for treating renal carcinoma, and in particular for preparing medicines for treating renal clear cell carcinoma.
US20120289567 Combinations of darifenacin and salivary stimulants for the treatment of overactive bladder Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of alleviating a side effect of treatment for overactive bladder in a patient suffering therefrom, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.
WO2012161559A2 A use of a composition comprising of acylated steryl glucoside in the manufacture of a product The present invention relates to a use of a composition in the manufacture of a product for regulating a plurality of genes consisting of phosphoenolpyruvate carboxykinase-1, fructose-1,6-bisphosphatase, xenobiotic metabolism, low-density lipoprotein receptor, apolipoprotein-A1, superoxide dismutase-2, and catalase, characterised in that: the composition comprising acylated steryl glucoside.
US20050053647 Pharmaceutical product comprising the active substance diamorphine, and its use in a process for treating opiate addiction The invention relates to pharmaceutical preparations that are used in a method for treating opiate addiction or opiate dependence, especially heroin dependence. The active substance used is preferably diamorphine and/or one of the pharmaceutically acceptable acid addition salts thereof. The invention also relates to a method for treating opiate dependence.
CA2192941C Sterol derivatives used for regulation of meiosis Certain sterols which can be extracted from bull testes and from human follicular fluid and chemically related sterols can be used for regulating the meiosis in oocytes and in male germ cells.
US20090181913 SPECIFIC GRP78 EXPRESSION-INHIBITION RNAi SEQUENCE, MEDICINE THEREOF AND METHOD THEREOF The present invention discloses a specific GRP78 expression-inhibition RNAi sequence, a medicine thereof and a method thereof, wherein an RNAi sequence 5′-AAGGATGGTTAATGATGCTGAGAA-3′ complementary to GRP78 forms a special hair-pin structure inside cancer cells to specifically and effectively inhibit GRP78 expression and then inhibit the canceration process, including the growth, migration, invasion, and metastasis of cancer.
CN101905000A Formula for treating rheumatism, method for preparing pills and medicinal liquor The invention discloses a formula for treating rheumatism, a method for preparing pills and medicinal liquor. The formula comprises 1 to 6g of Chinese angelica, 1 to 8g of szechuan lovage rhizome, 1 to 7g of liqouric root, 1 to 7g of cassia twig, 1 to 6g of rhizoma corydalis, 1 to 7g of notopterygium root, 1 to 6g of clematis, 1 to 8g of swordlike atractylodes rhizome, 2 to 9g of golden cypress, 1 to 6g of dried tangerine and 1 to 7g of achyranthes. The method for preparing the pills comprises the following steps of: packaging in a cloth bag, baking in an earthenware cooking pot, soaking in white spirit for 1 day, drying, grinding the mixture into powder, and honeying into the pills with spirit or water. Or based on the mixed medicament, a mixture of 2 to 4g of agaric, 2 to 5g of Japanese yam and 2 to 5g of moghania and 2 to 5g of Rhus semialata, two 0.5kg cobras, two 0.25-0.5kg long-noded pit vipers and two 0.25-0.5kg stink rat snakes are added, and soaked in white sprite for four months to prepare the medicinal liquor. The formula is a good formula for treating the rheumatism, which has the advantages of quicker response and capacity of treating both principal and secondary aspect of disease.
CN102068443B Compound florfenicol preparation for aquatic products and preparation method and application thereof The invention discloses a compound florfenicol preparation for aquatic products and a preparation method and application thereof. The compound florfenicol preparation for the aquatic products consists of the following components in percentage by mass: 5 to 20 percent of florfenicol, 1 to 25 percent of neomycin sulfate and the balance of glucose. The florfenicol and the neomycin sulfate are combined, so that the antibacterial effect of the compound florfenicol preparation for the aquatic products can be improved, the prevention and treatment effects of the compound florfenicol preparation on the bacterial diseases of the aquatic products are effectively improved, and medicine consumption and cost are reduced; and the preparation method of the compound florfenicol preparation for the aquatic products is simple and practicable and greatly improves bioavailability, and the preparation has high solubility.
EP1416923B1 Reduction of hair growth A topical composition for reduction in hair growth includes α-difluoromethylornithine and a dermatologically acceptable vehicle including urea.
WO2011062561A1 The isolation and characterisation of heparan sulphates and their use in pharmaceutical compositions, methods of treatment and stem cell culture media suitable for conditions associated with bone repair. Heparan sulphates isolated from male and female murine liver, their characterisation and use in pharmaceutical compositions, methods of treatment and in stem cell culture media suitable for conditions associated with bone repair.
WO2014084246A1 Inhibitor of nucleic acid for regulating activity of rnai molecule The purpose of the present invention is to provide a chemical capable of controlling a specific nucleic acid for regulating the activity of an RNAi molecule. Provided is an inhibitor of a nucleic acid for regulating the activity of an RNAi molecule, said inhibitor comprising a nucleic acid molecule that contains a base sequence being completely or sufficiently complementary to the base sequence of the single-stranded nucleic acid moiety of the target nucleic acid for regulating the activity of an RNAi molecule and, moreover, a base sequence being completely or sufficiently complementary to the base sequence of the double-stranded nucleic acid moiety thereof, and comprises at least DNA.
US20090238797 Nicotine-carrier vaccine formulation The present invention is in the fields of medicine, public health, vaccine and drug formulation. The invention provides composition formulations comprising a nicotine-carrier conjugate and a stabilizer, wherein said stabilizer comprises a non-reducing disaccharide and a non-ionic surfactant. The composition formulations are stable after a long time of storage at room temperature.
WO2007039201A2 Photostable pharmaceutical composition containing brivudine for the treatment of herpetic keratitis Ophthalmic composition containing brivudine as active ingredient and a film-forming agent selected from the group consisting of polyvinyl pyrrolidone (PVP), polyvinyl alcohol (PVA) and polyacrylate (PA).
WO2009136611A1 Glutathione production enhancer, prophylactic/therapeutic agent for diseases associated with lack of glutathione, and food, beverage and feed The object aims to find a substance having a glutathione production-enhancing activity among highly safe natural substances and to provide a glutathione production enhancer and a prophylactic/therapeutic agent for diseases associated with the lack of glutathione each of which comprises the substance as an active ingredient. The glutathione production enhancer or the prophylactic/therapeutic agent for diseases associated with the lack of glutathione comprises, as an active ingredient, a licorice extract composition which contains liquiritin, liquiritigenin, isoliquiritin and isoliquiritigenin but does not substantially contain glycyrrhetinic acid.
EP2228062A1 Compositions containing a phospholipid-curcumin complex and piperine as chemosensitizing agent This invention relates to compositions containing curcumin in phospholipid-complexed form and piperine with chemosensitising action for the treatment of drug resistance.
EP1687298A1 Cycloalkyl derivatives of 3-hydroxy-4-pyridinones The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula (I); wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R 2 R 5 N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups. X is C3-C6 cycloalkyl; Y is selected from the group consisting of C1 to C6 cycloalkyl; C1 to C6 alkyl, and C1 to C6 alkyl monosubstituted with a C3-C6 cycloalkyl; T is C1 to C6 alkyl; W is C3-C6 cycloalkyl; R3 is selected from the group consisting of hydrogen and C1 to C6 alkyl; R4 is selected from the group consisting of hydrogen and C1 to C6 alkyl; R5 is selected from the group consisting of hydrogen and C1 to C6 alkyl; and its pharmaceutically acceptable salt thereof. Pharmaceutical compositions of such compounds are useful in the removal of excess body iron from patients with iron overload diseases.
EP2353591A1 Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof The invention refers to a combination comprising a sigma ligand of formula (I) and an opioid or opiate for use in the prevention and/or treatment of pain developed as a consequence of surgery, especially peripheral neuropathic pain, allodynia, causalgia, hyperalgesia, hyperesthesia, hyperpathia, neuralgia, neuritis or neuropathy. The invention also refers to the sigma ligands of formula (I) for use in potentiating the analgesic effect of an opioid or opiate and/or for decreasing the dependency induced thereby when said opioid or opiate is used in the prevention and/or treatment of pain developed as a consequence of surgery.
US8013011 Topically applying artemisinine and/or one or more structurally related compounds; dermatomycosis A method of treating a benign pigmented mole or a dermatomycosis. The method comprises locally applying to a subject in need thereof artemisinine and/or one or more structurally related compounds. Also disclosed is a plaster which comprises a topical formulation comprising artemisinine and/or one or more structurally related compounds.
CN103360447A Macrolide solid-state forms This invention relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.
CN102617588A Anti-tumor compound, and preparation method and application thereof The invention discloses an anti-tumor compound, and a preparation method and application thereof. According to the anti-tumor compound, a structural formula is shown as a formula I. The compound LS1924A belongs to a compound with a new structure, and has high anti-tumor activity, and is suitable for the study of anti-tumor lead compounds or the preparation of anti-tumor medicines.
CN102091081A Composition for preventing or treating apoplexy and application thereof The invention relates to a composition for preventing or treating apoplexy and a preparation method thereof, wherein the composition comprises the following components in parts by weight: 4.8-10 parts of notoginsenoside R1, 19.8-45 parts of ginsenoside Rg1, 20-40 parts of ginsenoside Rb1, 3.5-6 parts of ginsenoside Re and 1.5-9.9 parts of ginsenoside Rd. The composition provided by the invention has the advantages of obvious effect and high safety and can obviously shorten the course of the disease and relieve the pain.
WO2005116015A1 Chromanol derivatives, method for the production thereof, and use thereof as an anti-inflammatory drug The invention relates to compounds of formula (I), a method for the production thereof, and the use thereof as an anti-inflammatory drug.
CN101704866A Rutin aliphatic ester derivatives, preparation method and application thereof The invention provides rutin aliphatic ester derivatives, which are prepared by chemically synthesizing rutin and the aliphatic ester. The rutin aliphatic ester derivatives have an easily-obtained raw material, low cost, simple preparation method and high yield, and are suitable for industrialized production. The pharmacological test shows that the rutin aliphatic ester derivatives have obvious effect for inhibiting platelet aggregation and inhibiting the activity of hepatitis virus, and can be used for preparing an anti-angiocardiopathy medicine, an anti-cerebrovascular disease medicine, an anti-viral hepatitis B medicine and an anti-hepatitis C medicine.
EP2746396A1 Selective local inhibition of TNFR1-mediated functions at the site of antigen/allergen presentation The invention relates to a pharmaceutical composition for the modulation of T cell and B cell responses made of one or more prepatations and comprising a therapeutically effective dose of at least one inhibitor of TNFR1-mediated functions and of at least one antigen or allergen.
WO2009045309A3 Use of v2 receptor antagonists in combination with vasopressinergic agonists The combination of vasopressin V2 receptor antagonists and vasopressin receptor agonists (selective or non-selective) is described, including pharmaceutical compositions, including kits, for administering, and methods and uses of such a combination, e.g. for treatment of critical care diseases and conditions requiring control of arterial blood pressure or for treatment of hypotension. Also described is the use of a combination of a vasopressin V2 receptor antagonist with a vasopressin receptor agonist for the manufacture of a medicament for treatment of critical care conditions requiring control of arterial blood pressure, vascular leak and/or vasodilation, methods for treatment of a critical care condition in a mammal needing control of arterial blood pressure, vascular leak and/or vasodilation, the method comprising administering to the mammal a therapeutically effective amount of a vasopressin V2 receptor antagonist and administering to the mammal a therapeutically effective amount of a vasopressin receptor agonist, and a kit comprising a therapeutically effective amount of one or more vasopressin V2 receptor antagonists in a pharmaceutically acceptable composition and a therapeutically effective amount one or more vasopressin receptor agonists in a pharmaceutically acceptable composition.
CN1785189A Method for quality control of compounding metformin glipidide A quality control method for compound flumamine glipizide includes such steps as examining its characteristics, identification by two characteristic reactions and thin-layer identification, and measuring the contents of flumamine hydrochloride, glipizide and cinnamaldehyde.
US20100292257 Uses of 2-[piperidinyl] methyl-2, 3-dihydroimidazo [1,2-c] quinazolin-5 (6h)-one for providing an analgesic effect, anti-allergic effect and histamine h1 receptor antagonism effect The present invention discloses new uses of 2-[piperidinyl]methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-one in providing an analgesic effect in a patient, treating passive cutaneous anaphylaxis in a patient, and in eliciting a histamine H1 receptor antagonism effect in a patient to treat a disease or disorder, such as allergy.
CN102526000A Dexibuprofen slow-release capsule and production method thereof The invention discloses a dexibuprofen slow-release capsule. Pellets are filled in the capsule, each pellet consists of a pellet core and four layers of materials wrapped outside the pellet core, the four layers of materials are sequentially an inner isolation layer, a first coating layer, a second coating layer and a third coating layer from inside to outside, and the pellet core, the inner isolation layer, the first coating layer, the second coating layer and the third coating layer respectively have the following compositions: the pellet core is prepared by medicine auxiliary materials, the inner isolation layer is stearic acid, the first coating layer is a coating mixture, the second coating layer comprises the coating mixture and the stearic acid, the third coating layer is the coating mixture, and the coating mixture consists of dexibuprofen and polyvidone K30. The invention also provides a production method of the dexibuprofen slow-release capsule. Compared with an ordinary capsule, the dexibuprofen slow-release capsule disclosed by the invention has the same absorption degree, but the dexibuprofen blood maximum concentration (Cmax) of the dexibuprofen slow-release capsule disclosed by the invention in human bodies is lower, the maximum time (Tmax) from the administration to the blood Cmax reaching is longer, and a good slow release effect is realized.
WO2011083314A1 Benzazepine derivatives for the treatment of central nervous system disorders A compound of the formula (1): wherein R1 represents C1-6 alkyl or H; Y represents -NR2R3 as depicted in formula (B), or a ring of formula (A) whereina represents the point of attachment to the pyrimidinyl ring; R2 represents C1-4halkyI substituted by C1-3 alkoxy; R3 represents C1-4 alkyl; W represents - (CH2)n-; W1 represents -(CH2)P-; n represents 1 or 2 or 3; p represents 1 or 2; R4 represents C1-4 alkoxy, C1-6 alkyl or halogen; and R5 represents halogen or H, provided that, when R4 represents halogen, R5 is not H, or a pharmaceutically acceptable salt thereof, is provided. The compounds of the invention have been found to modulate the histamine H3 receptor.
EP0946221B1 Use of taurolidine or taurultam for the prevention and the treatment of infections in delivery systems The use of taurolidine or taurultam in a method of combatting infection or sepsis in delivery systems is disclosed. In the method, taurolidine or taurultam solutions are used as a temporary seal or flush to prevent or reduce sepsis in delivery systems, such as port systems and/or catheters by which liquids are delivered into a patient.
EP2254567A2 Novel use of zinc n-acetyltaurinate The subject matter of the present invention is Zn N-acetyltaurinate of formula: [CH3-CO-NH-CH2-CH2-SO3]2 - Zn2+ for preventing and/or treating diseases with lipofuscin accumulation due in particular to ageing or to oxidative stress, and for preparing a medicament that is of use in treating these diseases. Use: treatment of diseases related to ageing or to oxidative stress, in particular age-related macular degeneration and diabetic retinopathy.
CN102343099B Preparation method and application of folacin mediated tumor targeting adriamycin prodrugs The invention provides a preparation method and application of two types of adriamycin prodrugs. The two types of prodrugs with tumor active targeting and acid-sensitive initial burst release properties can be prepared by virtue of connection of hydrazone bonds and introduction of folacin. By utilizing the two types of prodrugs, the tumor resistance of adriamycin can be reinforced, the toxic and side effects of the medicament can be reduced, and the targeting property can be improved. Therefore, the preparation method provides a novel idea for the development of anti-tumor medicaments.
US7541373 2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl} acetic acid; 2-[3-(4-Methyl-2-[2-methylpropoxy] phenyl)-ureido]-thiazol-4-yl}-acetic acid; activators of glucokinase; treatment of metabolic disorders, hyperglycemic agent, syndrome x, anticholesterol, hypertension etc. This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
CN103463117A Applications of drug composition of rubescensin and etoposide in preparation of antitumor drugs The invention discloses applications of a drug composition in treatment of tumor and preparation of antitumor drugs, wherein the major ingredients of the drug composition are rubescensin and etoposide (also known as VP-16). According to the drug composition, rubescensin and etoposide, which possess different action mechanisms, are combined, so that the tolerance of cells, which are insensitive to apoptosis, against etoposide is eliminated, and inhibiting and killing effects on tumor cells are improved greatly. Proliferation inhibiting and apoptosis inducing effects of the combination of rubescensin and etoposide are better than that of simply adding the effects of independent utilization of rubescensin and etoposide together. Therefore the drug composition is capable of realizing dosage reduction of rubescensin and etoposide with preferable antitumous effect being maintained. The antitumor drug composition with high efficiency low toxicity can be used for treatment of a plurality of kinds of malignant tumors, especially for treatment of leukemia, and tumour with tolerance aganist etoposide.
CN102304047A Gamma-hydroxy olic acid ester derivatives and use thereof in preparation of antitumor medicines The invention discloses gamma-hydroxy olic acid ester derivatives having antitumor activity and the use thereof in the preparation of antitumor medicines, and belongs to the field of biochemical technology. The structure of the gamma-hydroxy olic acid ester derivatives is shown below. The results of classic methyl thiazolyl tetrazolium (MTT) tumor cell medicine screening experiments, AnnexinV/PI double-staining cell apoptosis measurement experiments, cell periodical detection experiments and in-vivo antitumor experiments prove that the gamma-hydroxy olic acid ester derivatives have proliferation inhibition effects on breast cancer, bladder cancer and liver cancer and can be used in the preparation of antitumor medicines as an active ingredient.
WO2014047715A1 Treatment of pulmonary surfactant dysfunction using cholesterol-sequestering cyclodextrins The use of cholesterol-sequestering agents, such as methyl-beta-cyclodextrin, for the treatment of pulmonary surfactant dysfunction is disclosed. It was discovered that oxidative damage to pulmonary surfactant arises due to the interaction between reactive oxygen species and cholesterol. Thus, by removing cholesterol from pulmonary7 surfactant through the addition of a cholesterol-sequestering agent, oxidative damage to the surfactant is mitigated. It was also shown that methyl-beta-cyclodextrin can restore normal function to dysfunctional surfactant removed from the lungs of children with cystic fibrosis and non cystic fibrosis bronchiolitis.
CN101433552A External-use medicament for treating psora The invention relates to an external used medicine for treating scabies, which is ointment obtained by using sublimed sulfur, realgar, borneol, camphor, mercurous chloride, tetracycline powder and dexamethasone powder as raw material drugs, crushing the raw material drugs into fine powder, adding vaseline into the fine powder and stirring the mixture evenly, and sterilizing the mixture. The ointment for treating the scabies has the function of quick healing, does not leave any sequela, has no any toxic side effect and anaphylactic reaction, is simple and practical to use, costs low, and can be generally accepted by patients. Through clinical experiments on 1,000 cases of scabies patients, all the scabies patients are healed, so the cure rate reaches 100 percent.
WO2009132593A1 Quinoline compounds, pharmaceutical compositions, preparation methods and uses thereof Quinoline compounds represented by formula A, pharmaceutically acceptable solvates, optical isomers or polymorphs thereof, wherein X is S or O, M is H, Na+, NH4 + or Ca2+; each of R1, R2 and R3 is independently H, halo, the substituent represented by formula D or E; R is H, halo, C1-C4 alkyl or C1-C4 alkoxy. Also disclosed are the pharmaceutical compositions and preparation methods of these compounds and the uses of these compounds for the manufacture of medicaments for inhibiting HMG CoA reductase or for the treatment and prophylaxis of the diseases which can be treated effectively by inhibiting HMG CoA reductase. The present quinoline compounds and their pharmaceutical compositions have an excellent lipid reduction effect in vivo and can be used for the treatment of the diseases relating to hyperlipidemia.
CA2402652C Viscoelastics for use in middle ear surgery Disclosed are viscoelastic compositions and methods of their use in surgical and non-surgical packing and in effecting drug delivery, especially in conjunction with trauma to or disorders of the ear.
CN102961390A Ophthalmic gel medicinal composition and preparation method thereof The invention discloses an ophthalmic gel medicinal composition and a preparation method thereof. The medicinal composition containing tobramycin and dexamethasone, disclosed by the invention, has the effect of treating anterior uveitis and keratitis; the ophthalmic gel medicinal composition is prepared through a scientific and reasonable production process; and the product is definite in function, controllable in quality and safe to take. The preparation method of the medicinal composition is simple, and the preparation process can be finished by conventional equipment.
CN101724045A Human epididymis expression sperm binding protein HEL-169 as well as encoding gene and application thereof The invention belongs to biotechnology and medical field and discloses a new human epididymis special expression sperm binding protein HEL-169 and preparation and application thereof. The invention discloses an amino acid sequence of the HEL-169 protein and provides a recombination expression vector carrying a DNA sequence for encoding the protein. The invention further discloses a method for preparing and detecting the protein. The protein is positioned at the perforatorium region of a sperm, an RT-PCR result shows that the protein has micro-expression mainly in epididymis and spermary. A band of about 20 KD is detected in the epididymis by using Western blot. The HEL-169 protein can be used as target protein for the research and development of immunity acyeterion as well as the clinical diagnosis and treatment of male infertility. A method for detecting corresponding gene or protein based on the protein HEL-169 can be widely applied to the reproductive medicine research field.
US7087634 Cyclic AMP-specific phosphodiesterase inhibitors Pyrazole compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
CN101380311B Diabecron sustained-release tablet and preparation method thereof The invention discloses a metformin hydrochloride slow release tablet which is prepared from the following materials according to the weight proportion: 68% of metformin hydrochloride, 18-22% of a slow release material and the residual amount of a pharmaceutic adjuvant, wherein, the slow release material takes the compound of hydroxypropyl methylcellulose K100 and glyceryl behenate, and the weight ratio of the hydroxypropyl methylcellulose K100 and the glyceryl behenate is 1:0.1-0.5. The metformin hydrochloride slow release tablet has the advantages of small in vitro release difference among tablets and batches, good curative effect, long drug action, little side effect, few administration frequency, convenient use and the like, and has unique advantages of treating and relieving type II diabetes symptoms, preventing sudden onset of diseases, protecting the daily life of patients and bringing the patients through the onset peaks; and the slow release provides reliable measures and great convenience for the treatment of the patients and self prevention of the sudden onset of diseases.
CN103536574A Coenzyme Q10 soft capsule and preparation method thereof The invention relates to a coenzyme Q10 soft capsule and a preparation method thereof. The coenzyme Q10 soft capsule comprises the following components by mass percentage: 1-20 parts of coenzyme Q10, 30-95 parts of diluent, 1-50 parts of emulsifying agent and 1-30 parts of cosolvent. The invention also provides a preparation method of the coenzyme Q10 soft capsule. The coenzyme Q10 soft capsule not only has high stability but also achieves excellent effects in product dissolvability and content uniformity; as phosphatide is used as an emulsifying agent, the emulsified coenzyme Q10 soft capsule has higher stability and water in vivo and lipid substances can be fully mixed so as to improve the bioavailability of a medicament.
EP2751107A1 Compounds and compositions as pdgfr kinase inhibitors The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of PDGFR (PDGFRα, PDGFRβ) kinases or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.
US20120208843 Method of Using GPR35 to Identify Metabolic-Stabilizing Compounds The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to a method for treating or preventing a metabolic-related disorder, comprising administering to an individual in need thereof an effective amount of a GPR35 modulator.
US20120183625 Method for preparing aqueous solution of high-concentration calcium phosphate stable in neutral ph range Disclosed herein is a method for preparing an aqueous solution of high-concentration calcium phosphate, the method comprising the steps of: preparing an acidic aqueous solution using an acidic chelating agent; and dissolving a calcium phosphate-based compound in the acidic aqueous solution, and then adding a pH-adjusting agent to the acidic aqueous solution to adjust the pH of the acidic aqueous solution. The disclosed aqueous solution does not form a precipitate after neutralization so that it can be used in various calcium-containing products, including foods, drugs, or quasi-drugs.
CA2161138C Oxidation products of cephalomannine Antineoplastic taxol derivatives are derived by selective oxidation of the alkene portion of the side chain of cephalomannine. The derivative displays high activity in promoting assembly of microtubulin and also displays cytotoxic activity against malignant cells.
US20090048259 Phthalazine compounds, compositions and methods of use The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.
CN101347416A Capsules type acetaminopher drop and method of preparing the same The invention relates to a capsule acetaminophen drop and a preparation method thereof in the technical field of medicines. A soft capsule is like a bottle gourd or fish and is composed of drop components and a soft capsule shell. The drop components comprise the acetaminophen, a dissolvent, a corrective and a pH regulator. The soft capsule shell consists of one or a plurality of gelatin, glycerol, water, pigment, an opacifier, a preservative and a disintegrating agent. The preparation method comprises the steps as follows: the acetaminophen, the dissolvent, the correctives and the pH regulator are mixed and dissolved at the temperature of 60-90 DEG C; the water and the glycerol are heated to the temperature of 70-90 DEG C, with one or a plurality of the gelatin, the preservative, the pigment, the opacifier and the disintegrating agent added while stirring to totally melt the gelatin, decompression is performed to remove bubbles in the gelatin solution, and heat preservation is carried out; the drop components are led to a soft capsule pellet press to prepare the soft capsule. The capsule acetaminophen drop has simple technology, beautiful appearance, controllable dosage, and is easily swallowed and good for storage.
CN103044311A Multi-substituted indole compounds and preparation method and application thereof The invention belongs to the technical field of medicines and particularly discloses multi-substituted indole compounds shown as a general formula I, FORMULA I (refer to the specification), and a preparation method thereof as well as application of compositions containing one or more multi-substituted indole compounds to anticancer medicines.
EP1853601B1 Non steroidal glucocorticoid receptor modulators The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. In this formula R1 is H or (1-4C)alkyl; R2 is -C(O)R15 or -S(O)2R15; R3 is H, (1-4C)alkyl or -OR16; R4 is H, (1-4C)alkyl or -OR16; R6 is H or -C(H)NOR16; R7 is H or halogen, cyano; (1-6C)alkyl, (2-6C)alkenyl or (2- 6C)alkynyl, all three optionally substituted with OH, halogen or NH2 ;-C(H)NOR16, - OR16, -C(O)R16, or -C(O)OR16; R8 is H, cyano, halogen, nitro; (1-6C) alkyl, (2- 6C)alkenyl, (2-6C)alkynyl or -O(1-6C)alkyl, all optionally substituted with amino, hydroxyl or halogen; (hetero)aryl, optionally substituted with cyano, halogen, (1- 4C)alkyl, (1-4C)alkoxy, (1-4C)alkoxy(1-4C)alkyl; -C(O)R18, -C(O)OR19, -C(O)NHR17, -NHC(O)R20, -C(1-4C)alkylNOR21; -C(H)NOR16, or -NHS(O)2R21; R9 is H, halogen, cyano or (1-4C)alkyl optionally substituted with halogen; R10 is H or (1-4C)alkyl; R11 is H; R12 is H, cyano or (1-4C)alkyl; R13 is H, (1-4C)alkyl, halogen or formyl; R14 is H, halogen, cyano, (1-4C)alkyl, (2-6C)alkenyl, C(O)R21 or (hetero)aryl; R15 is H; (1- 6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl,-O(2-6C)alkyl, -O(2-6C)alkenyl or -O(2- 6C)alkynyl, all optionally substituted with one or more OH, halogen, cyano or (hetero)aryl, (hetero)aryl, optionally substituted with (1-4C)alkyl, halogen, cyano, nitro or amino, NH2, (di)(1-4C)alkylamino, (1-4C)alkyl(1-4C)alkoxyamine, (1- 4C)alkylt hio(1-4C)alkyl or (1-4C)alkoxy(1-4C)alkyl; R16 is H, (1-6C)alkyl, (2- 6C)alkenyl or (2-6C)alkynyl; R17 is H, (1-6C)alkyl, optionally substituted with halogen, (1-4C)alkoxy or (hetero)aryl, optionally substituted with halogen, (1-4C)alkyl or (1- 25 4C)alkoxy; (3-6C)cycloalkyl or (hetero)aryl, optio nally substituted with halogen, (1- 4C)alkyl or (1-4C)alkoxy; R18 is H, NH2, C(O)R21 or (1-4C)alkyl, optionally substituted with OH, halogen, cyano or -S(1-4C)alkyl; R19 is H or (1-6C)alkyl, optionally substituted with OH or halogen; R20 is H, (1-6C)alkyl or (2-6C)alkenyl, both optionally substituted by halogen, O(1-6C)alkyl, (hetero)aryl, optionally substituted with (1- 4C)alkyl or halogen; (3-6C)cycloalkyl; (1-6C)alkoxy; (1-6C)alkenyloxy; or (hetero)aryl, optionally subst ituted with (1-4C)alkyl); NH2, -NH(1-6C)alkyl or -NH(hetero)aryl and R21 is H or (1-6C)alkyl. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.
CN1850056A Taxotere lyophilized powder and its preparing method The present invention relates to an antitumor medicine docetaxel freeze-dried powder injection and its preparation method. Said invention also provides the concrete steps of its preparation method.
US7329654 Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.
US20130034537 Simultaneous co-treatment of physical and mental symptoms related to severe mental disorders by a specially fermented soy formulation (fsww08) A method of treating severe mental diseases and related disorders or conditions includes administering to a patient in need thereof an effective amount of a composition including isoflavones and Bowman Birk Inhibitory Factor (BBIF). Preferably, the composition is a fermented soy composition. Preferably, one first diagnoses a patient with a particular mental disease or disorder, and then prescribes the composition as a treatment for the particular mental disease or disorder. A patient is preferably given daily a dosage of 3-10 mg of isoflavones and 5-10 Cl (chymotrypsin inhibitor) of BBIF per kg of body weight, more preferably a dosage of 5-9 mg of isoflavones and 5-10 CCl of BBIF per kg of body weight, and most preferably a dosage of 5-10 mg of isoflavones and 5-10 CCl of BBIF per kg of body weight. Treatment preferably lasts 7 days-14 days, or until all symptoms disappear.
WO2009125597A1 Acylthiourea compound or salt thereof, and use of the compound or the salt Disclosed is an anti-tumor agent which has an excellent inhibitory activity on c-Met, can selectively act on a tumor cell in which c-Met is expressed specifically, and has reduced adverse side effects. Specifically disclosed is an acylthiourea compound represented by general formula (I) [wherein R1 and R2 independently represent a hydrogen, an alkyl group, a cyclioalkyl group, an aromatic hydrocarbon group or a saturated or unsaturated heterocyclic ring, or R1 and R2 may together form a ring; R3 represents a C1-6 alkyl group; and R4, R5 and R6 independently represent a hydrogen, an alkyl group, an alkoxy group, an alkylamino group, an aromatic hydrocarbon group, a saturated or unsaturated heterocyclic ring or the like] or a salt thereof.
US20100291069 Methods of treating a diabetic embryopathy Maternal diabetes can lead to a developmental malformation of an embryo. A developmental malformation caused by maternal diabetes is commonly referred to as a diabetic embryopathy. There is currently no effective treatment for reducing or inhibiting a diabetic embryopathy. To this end, the present invention is drawn to novel methods of treating a diabetic embryopathy.
WO2011096377A1 Pyrrole compound Disclosed is a novel low molecular weight compound that has an immunosuppressive effect. Specifically disclosed is a compound represented by general formula (I) or a pharmacologically acceptable salt thereof. (In the formula, substituents are defined as follows: R1 and R2 each represents a hydrogen atom or the like; R3 represents a hydrogen atom or the like; m represents 0 or the like; Y represents an ethylene group or the like; Z represents a single bond or the like; and R4 represents a hydrogen atom or the like.)
CN102887887A 2-(1-substituted piperidine-4-amino)-6-(substituted phenylamine/phenol) pyridine derivatives and preparation method and application thereof The invention relates to 2-(1-substituted piperidine-4-amino)-6-(substituted phenylamine/phenol) pyridine derivatives and a preparation method and application thereof. R1 represents CH3, CN and (E)-cyanovinyl; X represents O, NH, S and CH2; R2 represents NO2, NH2, CN, halogen, H, OH, COOH, CONH2, SO2NH2 and SO2CH3; n is 0 or 1; and Ar is phenyl, 4-pyridyl or single-substituted or multi-substituted phenyl at ortho-position, meta-position and para-position. The invention also relates to the application of the compound in preventing and treating HIV (human immunodeficiency virus) infection.
EP2575823A1 3-substituted vinylboronates and uses thereof 3-substituted vinylboronates and their use in the treatment of cancer such as colorectal cancer are disclosed. In some embodiments, the 3-substituted vinylboronates have the general Formula I: (see formula) with the variables in the formula being as defined in the specification.
CN103044391A High-efficient DPP (dipeptidyl peptidase)-IV inhibitor The invention belongs to the technical field of medicines, relates to a high-efficient DPP (dipeptidyl peptidase)-IV inhibitor, and specifically relates to a compound taking uracil as a mother nucleus, or a salt thereof, a preparation method, a composition and an application of the compound as the DPP-IV inhibitor in prevention or treatment of diseases which benefit from DPP-IV inhibition. The compound disclosed by the invention has a very good selective inhibition effect against DPP-IV and has very low cardiotoxicity, thereby being a DPP-IV inhibitor type medicament with great prospects.
US20110184015 Novel derivatives of pyrroloindole which are inhibitors of hsp90, compositions containing same, and use thereof Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R′1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1,2 and m=0, 1; R1 and/or R′1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being in all isomer forms and salts, as medicaments.
CN1810827A Anticancer prepn containing three anticancer compounds of toad or toad cake and its prepn process The present invention is several kinds of toad preparations for treating tumor and their preparation process. Toad or toad cake is extracted and refined to prepare medicine preparations in different forms. Compared with available technology, the present invention has simple extraction and separation process and is reasonable and practical, and the preparations have reliable curative effect. The toad preparations have the functions of killing tumor cell, inducing tumor cell differentiation and death, inhibiting tumor cell vascularization, etc. and are used in treating primary liver cancer, lung cancer in medium and later stage, breast carcinoma and other tumors.
WO2008089307A3 Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer This invention relates to methods of treating, managing and preventing pain, inflammation, cancer, and ocular diseases and disorders, and to compounds and pharmaceutical compositions useful in such methods.
US7837987 Fusion using polyoxyalkylene glycol To achieve, an in vivo repair of injured mammalian nerve tissue, an effective amount of a biomembrane fusion agent is administered to the injured nerve tissue. The application of the biomembrane fusion agent may be preformed by directly contacting the agent with the nerve tissue at the site of the injury. Alternatively, the biomembrane fusion agent is delivered to the site of the injury through the blood supply after administration of the biomembrane fusion agent to the patient. The administration is preferably by parenteral administration including intravascular, intramuscular, subcutaneous, or intraperitoneal injection of an effective quantity of the biomembrane fusion agent so that an effective amount is delivered to the site of the nerve tissue injury.
WO2011076711A3 Polymorphs of salts of 4- [4- [ [4-chloro-3- (trifluoromethyl) phenyl] carbamoylamino] phenoxy] -n-methylpyridine - 2 - carboxamide The present invention relates to polymorphs of 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]- carbamoylamino]phenoxy]-N-methyl-pyridine-2-carboxamide.
EP2114904A1 Antifungal triazole derivatives, method for the preparation thereof and pharmaceutical composition containing same The present invention relates to triazole derivaties, a method for the preparation thereof, and a pharmaceutical composition containing the same as an active ingredient. The inventive triazole derivaties have an excellent antifungal activity against various pathogens.
WO2008070009A3 Treating solid tumors and monocytic leukemia using topoisomerase inhibitors in liposomes A method of treating a solid tumor or leukemia is described. More specifically, a method of treating a solid tumor or leukemia with liposome-entrapped topoisomerase inhibitor is provided. In one embodiment, the method involves treating leukemia by evaluating a subject's monocytes and/or neutrophils, and administering at least one topoisomerase inhibitor entrapped in liposomes having an outer surface coating of hydrophilic polymer chains based upon the evaluation. In another embodiment, the method involves treating a solid tumor, by selecting a treatment regimen based on the age and/or ratio of total body weight to ideal body weigh of the patient.
US20080132445 increasing milk production; inhibiting tumors; administering Galanin with prolactin; transgenic mammal The present invention relates to compositions and methods for inducing mammary epithelial cell differentiation in mammalian subjects. More specifically, the present invention relates to methods for inducing mammary epithelial cell differentiation which comprise increasing the levels of galanin in the mammary tissue of the subject. In one aspect the present invention relates to a method of increasing milk production in a lactating mammal which comprises increasing the level of galanin or an analog thereof in the mammal. In another aspect the present invention relates to a method of enhancing mammary development in a mammal, the method comprising administering to the mammal galanin or an analog thereof in conjunction with prolactin or an analog thereof. In yet another aspect the present invention relates to a method for inhibiting mammary epithelial tumours by administering an inhibitorially effective therapeutic amount of galanin or an analog thereof.
CN103315959A Orally taken colon-targeted preparation for treatment of inflammatory bowel diseases and preparation method thereof Belonging to the field of medicinal preparations, the invention relates to an orally taken colon-targeted preparation for treatment of inflammatory bowel diseases, particularly to an Eudragit S100 wrapped 5-aminosalicylic acid nanoparticle and its preparation method. In the invention, 5-aminosalicylic acid is taken as a model drug, and a pH sensitive Eudragit S100 is employed as a coating material to prepare the Eudragit S100 wrapped 5-aminosalicylic acid nanoparticle with a particle size of 70-400nm. The prepared nanoparticle can protect a 1, 5-aminosalicylic acid drug from being damaged by the digestive juice in a gastrointestinal tract until the drug reaches a colon region with pH greater than 7. The preparation method provided in the invention is simple to operate, and the prepared colon-targeted nanoparticle has the characteristics of small particle size and narrow distribution, as well as low solvent residue. The orally taken colon-targeted preparation can be used as a novel preparation of 5-aminosalicylic acid in treatment of inflammatory bowel diseases.
CN100998568A Benda-lysine oral disintegrant tablet and its preparing method An oral disintegrating tablet of bendalysine is proportionally prepared from bendalysine, filler, disintegrant and lubricant through respective sieving, proportional mixing and tabletting.
EP1864663A1 Preventive and/or therapeutic agent for rheumatoid arthritis The present invention relates to a preventive and/or therapeutic agent for rheumatoid arthritis. The present invention provides a preventive and/or therapeutic agent for rheumatoid arthritis containing 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H-pyr idazin-3-one and a COX2 inhibitor.
CN1582929A Aparkan drops and their preparation A dripping pill of trihexyphenidyl is prepared by superfine pulverizing and conventional process for preparing dripping pills.
WO2014024168A1 Polymeric crown ether derivatives used in the treatment of proliferative diseases, in particular cancer The present invention relates to a polymeric crown ether derivative having the following formula (I): R1-[CH2-CH2-C(COO-L-CE)(COO-R3)]n-R2 (I) in which n is the average number of repeating units, between 2 and 80, R1 and R2 are independently end groups chosen from a hydrogen atom, an -S-phenyl group, a charged group and a hydrophilic polymer, R3 is a (C1-C20)alkyl group or an -L-CE group, CE is a crown ether unit, and L is a spacer, wherein said derivative of formula (I) is in any of the racemic, enantiomeric and diastereoisomeric isomer forms, for use thereof as a medicament. The present invention also relates to a pharmaceutical composition containing such a derivative, and to such a derivative for use thereof as a dermatological active agent.
CN101732703B Composition for antagonizing pyretic effect of endotoxin in vaccine on livestock and application thereof The invention discloses a composition for antagonizing pyretic effect of endotoxin in vaccine on livestock and application thereof. The composition consists of polymyxin B and glycin, wherein the concentration of the polymyxin B is 200mu g/ml; and the concentration of the glycin is 200mg/ml. A mouse is taken as a model, clinical manifestation of the mouse is observed after the polymyxin B and theglycin are jointly used for the vaccine, the fatal influence of the polymyxin B and the glycin on the mouse is observed, and the optimal mixture ratio of the PMB to the Gly for jointly antagonizing the endotoxin in the vaccine is determined, namely the composition is added to the vaccine until each milliliter of the vaccine contains 2 to 4 mu g of the polymyxin B and 20 to 40mg of the glycin; thecomposition has good endotoxin combining and neutralizing capacity, can effectively antagonize the endotoxin in the vaccine, and has the synergic antagonistic effect; in addition, the two antagonistsare simultaneously applied, and the consumption of a single antagonist is effectively reduced, so the toxic and side effect of the medicament is reduced.
US20080108695 5,6,7-trihydroxyheptanoic acid and its analogs ; allergic dermatitis, contact hypersensitivity, urticaria (hives), rosacea, or psoriasis The use of 5,6,7-trihydroxyheptanoic acid and analogs is disclosed for the treatment of asthma, allergic rhinitis, and skin disorders such as allergic dermatitis, contact hypersensitivity, urticaria (hives), rosacea, or psoriasis.
CN101269037A Esomeprazole magnesium sustained-release dropping pill and preparation method thereof The invention discloses a pharmaceutical preparation used for treating erosive reflux oesophagitis, a gastroesophageal reflux disease, maintaining a long-term therapy to prevent the recurrence of oesophagitis for a cured patient, controlling the symptoms of gastroesophageal reflux diseases, eradicating helicobacter pylori jointly medicated with an appropriate antimicrobial therapy, healing duodenal ulcer related to helicobacter pylori infections and preventing the recurrence of peptic ulcer related to helicobacter pylori, and particularly relates to a prepared sustained-release oral formulation adopting esomeprazole magnesium as the ingredient. The pharmaceutical preparation aims to supplement the deficiency of the prior art and provide a sustained-release esomeprazole magnesium dropping pill. The sustained-release esomeprazole magnesium dropping pill overcomes the defects in the prior art effectively, guarantees no occurrence of an obvious quality change for the drug during the effective storage period and has the advantages of controllable release time, full release and high bioavailability simultaneously.
WO2011112071A2 Synergistic effect of tocotrienols and curcumin The present invention relates to a transdermal fluid wherein the main ingredient is tocotrienol; and curcumin is added to enhance the anti-cancer effects of tocotrienols. The composition is useful for the treatment or prevention of a cancer or a tumour or an inflammatory disorder, particularly breast cancer.
CN1771970A Compound Western medicine prepn for treating respiratory tract diseases and its prepn The present invention is one kind of compound Western medicine preparation for treating respiratory tract diseases and its preparation. The compound Western medicine preparation is prepared with dioxopromethazine hydrochloride, benproperine phosphate and proper supplementary material, and is prepared into pharmaceutically acceptable preparation forms. The present invention has the synergistic effects of both dioxopromethazine hydrochloride and benproperine phosphate, and may be used to treating cough, asthma and phlegm, especially irritative dry cough.
CN103417566A Hydrogen-containing eye drops and preparation method and application thereof The invention discloses hydrogen-containing eye drops and a preparation method and application thereof. The hydrogen-containing eye drops comprise injection water and 0.5-1.3 mmol/l hydrogen. The preparation method of the hydrogen-containing eye drops includes: introducing hydrogen into the injection water in the tightness condition; after the hydrogen is dissolved and saturate in the injection water, stopping hydrogen introduction to obtain hydrogen-containing solution; filling and sealing to obtain the hydrogen-containing eye drops. The hydrogen-containing eye drops are applied to treating corneal neovascularization. The hydrogen-containing eye drops have the advantages that expression of an important VEGF (vascular endothelial growth factor) in corneal neovascularization growth factors is decreased by lowering inflammatory response factor interleukin-1 (IL-1) and tumor necrosis factor-alpha (TNF-alpha); secretion of MMPs (matrix metalloproteinases) can be inhibited, and accordingly less corneal neovascularization occurs, keratitis response is lessened, and great benefit is brought to patients with corneal neovascularization.
US20090209614 administering glutamine or glutamine chloride to a patient for increasing blood flow in in the capillary vessels; treating a condition selected from dementia, cold constitution, shoulder stiffness, skin muddiness, muscle fatigue, impaired liver function, lowered immunity The present invention provides a glutamine-containing composition which functions to increase blood flow. Glutamine is present in the composition in an amount of 25 mg/kg body weight to 150 mg/kg body weight. By administering the composition to a subject in need thereof, the blood flow in the capillary vessels can be efficiently increased, while inhibiting any side effects such as low blood pressure. The present invention also provides food or feed containing the composition for increasing blood flow.
US20100221746 Compositions and methods for the treatment of disease The present invention relates to pharmaceutical compositions for the treatment and/or prophylaxis of disease associated with fibrosis in a vertebrate, said composition comprising at least one activin antagonist, and optionally a pharmaceutically acceptable carrier, adjuvant and/or diluent. The invention also relates to methods of treatment of disease associated with fibrosis in a vertebrate, as well as methods for diagnosing such conditions, and kits therefor.
US7153884 C-2′ methylated derivatives of paclitaxel for use as antitumour agents Taxane derivatives of formula (I) in which: R is trifluoromethyl, phenyl, 2-furyl, 2-thienyl; R1 is t-butoxycarbonyl or benzoyl; R2 is hydroxy; R3 is hydrogen or, together with R2, it forms the residue of a cyclic carbonate of formula: II with the proviso that when R3 is hydrogen, R is different from phenyl. Compounds of formula (I) have antitumor activity
US8658645 Use of quinolone antibiotics The present invention relates to the use of certain quinolone antibiotics for controlling bacterial disorders of the oral cavity, in particular in veterinary medicine.
CN102746292A Cyclized berberine derivatives, preparation method and uses thereof The present invention relates to cyclized berberine derivatives, a preparation method and uses thereof. The present invention specifically relates to compounds represented by a formula I or a pharmaceutically-acceptable salt or a solvate thereof, wherein X is a halogen, R is selected from hydrogen, C1-6 alkyl, phenyl substituted C1-6 alkyl, C1-18 alkylacyl, benzoyl, benzenesulfonyl, and 3,4-C1-3alkylidene dioxybenzoyl, the phenyl is optionally substituted by 1-4 substituents selected from halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxy, C1-4 alkyl acylamino. The compounds of the present invention have beneficial physiological activities.
CN1923176A Oil-in-water baicalin nano-milk oral liquid and its preparing process The invention discloses an oil-in-water type baicalin nano milk oral liquid comprising surface active agent, oil, baicalin and distilled water. The preparing process comprises the steps of weighing surface active agent, mixing with co-surfactant, calculating HLB according to HLB of the surface active agent, proportioning ratio with the oil, charging distilled water at 20-25 deg C and stirring sufficiently, charging baicalin proportionally, stirring to fully dissolve the materials, forming stabilized yellow transparent system.
CN103695497A Enzymatic preparation of naloxone and pharmaceutical composition thereof The invention provides a method for enzymatic preparation of naloxone. The enzyme is mild in reaction condition and free of harm to a human body. In addition, the invention also provides a naloxone composition prepared by the method and application thereof. The composition contains 14-hydroxy-7,8-dihydro codein ketone impurities, but the medicine performance can not be affected. Furthermore, the invention also provides an identification method of the naloxone composition and enzyme and the like for preparation.
CN102451301A Externally-used paste for treating psoriasis The invention discloses externally-used paste for treating psoriasis, which comprises the following components: 20-40 g of purslane, 5-10 g of mints, 5-8 g of camphor, 10-15 g of grape seeds, 20-30 g of methotrexate cream, and 20-30 g of vaseline. The preparation method comprises the following steps: pulverizing mints, camphor, and grape seeds, sieving by a 200-mesh sieve, then adding methotrexate cream, well mixing; pulverizing fresh purslane to obtain thick liquid, adding the above components, then adding vaseline, well mixing to prepare paste. During treatment, the paste is applied to an affected part. The paste is only applied once a day, takes effect generally after three to four days, and takes obvious effect after two months when complete recovery is almost reached. During treatment, oral medicaments are simultaneously taken as well. Totally 245 patients are treated by the invention, and oral medicaments are combined for simultaneous administration generally during treatment; 202 patients are cured; the treatment is effective for 23 patients, and is ineffective for 20 patients; the total effective rate is up to 91.8%. The medicament of the invention has the advantages of good treatment effect, low cost, and the like.
US20110144033 Proteasome Inhibitors and Methods of Using the Same The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.
US20100152160 Novel benzodioxane and benzoxazine derivatives useful as cc chemokine receptor ligands The present invention relates to benzodioxane and benzoxazine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
US20080292607 Nutraceutical agent for attenuating the neurodegenerative process associated with Parkinson's disease This invention describes a comprehensive nutraceutical designed to antagonize major mitigating factors to the degenerative process associated with Parkinson's disease. The formulation is comprised of a primary base of pyruvate, succinate and/or oxaloacetate, fruit extracts and anthocyanins, further combined with specific macro/micronutrients, trace elements, amino acids, flavonoids and concentrated plant sources. The nutraceutical contains substances that should attenuate the loss of ATP/toxicity by PD model toxins: 1-methyl-4-phenylpyridinium and rotenone, scavenge hydrogen peroxide/O2.−, augment antioxidant enzymes, prevent dopamine (DA) oxidation to DA-quinone via inhibition of COX, PLA2, LOX, xanthine oxidase, tyrosinase, prevent hyperhomocysteinemia, antagonize PARP-1 apoptosis, increase blood flow, glucose and oxygen delivery to the brain, potentiate mitochondrial function, antagonize glia iNOS and MAO or its products, chelate redox-active iron, inhibit heme oxygenase-1, inhibit alpha-synuclein aggregation, augment ATP storage, mediate anti-inflammatory effects via inhibition of PDE, MAPK p38/c-Jun NH2-terminal kinase/PGE2, antagonize excitotoxicity and downregulate N-methyltransferase, all of which contribute toward PD pathology.
WO2007006543A1 Camptothecin analogues, process for their preparation, use and formulations containing them The present invention relates to novel camptothecin derivatives of general formula (I) in which R1 is a straight or branched polyamino residue, optionally functionalized by acylation or alkylation of the amino residues with more than 2 nitrogen atoms; R2 is H, -OR3; R3 is H or a straight or branched C1-C24 saturated or unsaturated acyl residue; R4 is H, straight or branched C1-C4 alkyl, hydroxyalkyl, aminoalkyl or cyano; R5 and R6 can be H, OH or OCH3. The compounds of the present invention can be conveniently administered for the therapy of tumors, in the form of suitable pharmaceutical formulations.
WO2010026602A2 Pharmaceutical compositions containing calcium channel blockers for treatment of tuberculosis The present invention provides calcium channel blockers for the treatment of drug sensitive and drug resistant Mycobacterium tuberculosis infection in humans and animals. In the present invention the role of L-type and R-type VGCC in M. tb infection in vitro and in vivo is disclosed. Inhibiting VGCC in DCs increases calcium influx and activates T cells that mediate killing of M. tb inside macrophages. Likewise, blocking VGCC in infected macrophages and PBMCs induces calcium influx and killing of M. tb. Blocking VGCC in vivo in M. tb infected mice using specific antibodies significantly reduces bacterial loads. Treatment of M. tb infected mice with conventional anti-TB drugs supplemented with a conventional calcium channel blockers such as amlodipine, S-amlodipine and nifedipine mediates a reduction in bacterial loads that is significantly better than drug treatment alone. In addition, these calcium channel blockers effectively kill single, multiple and extensively drug resistant stains of M. tb. Histology of spleen of different treatments indicates a marked improvement in granuloma composition with a significant decrease in cavity formation and restoration of protective granuloma architecture.
CN101708182A Application of troxerutin in preparing medicine resisting viral hepatitis The invention relates to a novel application of troxerutin in a medicine. By carrying out in-vitro and in-vivo pharmacological experiments of resisting hepatitis B viruses and hepatitis C viruses on the troxerutin, a result proves that the troxerutin has an obvious function of suppressing the hepatitis B viruses and the hepatitis C viruses. Therefore, the troxerutin can be used for preparing a medicine resisting viral hepatitis, especially for preparing a medicine resisting viral hepatitis B and viral hepatitis C. Moreover, the price of the required raw materials is low, the raw materials are easy to obtain, and the use in a large range is convenient.
CN101103961A Oral mixed suspension preparation The invention provides an oral suspension agent for treating dysuria, containing silodosin, an active ingredient, or salt acceptable in pharmacy, the prodrug of silodosin. The suspension agent can be a dry suspension agent easy for dispersion and hydration or a liquid suspension agent. The oral suspension agent of the invention has stable property and better adaptability, applicable for the elders.
WO2006125596A1 Organic compounds for the treatment of imflammatory or alleric conditions Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.
US20080255156 2-Phenyl-s-triazolo[4,3-c]quinazolin-3-one derivatives; neurodegenerative and central nervous system disorders; Parkinson's and Alzheimer's disease; restless leg syndrome; sleep, attention deficit, and psychological disorders; antidepressants; strokes, psychosis Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein: X1 and X2 are 1-3 substituents independently selected from the group consisting of H, alkyl, halo, —CF3, —OCF3, alkoxy, —OH and —CN; n is 0, 1 or 2; and R and R1 are H or alkyl; also disclosed is the use of the compounds in the treatment of CNS diseases such as Parkinson's disease, alone or in combination with other agents for treating CNS diseases, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
US7312336 Ligands for the delta opiod receptor; novel compounds which possess a piperidine ring with an exocyclic double bond do not show significant convulsive effects when administered systemically Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
CN1935849A Ultramicro chito polysaccharide product and its processing method The invention discloses ultr-fine chitosan products and its processing method. It includes the following steps: selecting chitosan solid particle with less than 200 mu meter diameter as raw material; adding edible vinegar by 10-50:1 weight ratio to infuse and mix; adding water to until pH value equals to 3-6; ultrasonic wave fine processing at the condition of 10-40 degree centigrade temperature, 10-100 Khz ultrasonic wave frequency, 100-1800 W power for 2-15m/ml for unit volume liquid to gain transparent liquid whose chitosan content is 0.1-20mg/ml, particle diameter is 0.25-100 nm; further processing to gain white powdery chitosan products with 1%-8% water content. The produced chitosan products can effectively increase active ingredient absorption ratio for people, using effect and stability in cancer prevention and against cancer.
CN102892765A New cyclohexylamine derivatives having [beta]2 adrenergic agonist and m3 muscarinic antagonist activities The present invention relates to novel compounds having [beta]2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
CN1994294A Use of plant extract catechin in preparation of antivirus medicine The invention relates to method for using plant extractive catechin to prepare drug, wherein it uses green tea extractive as material; extracts in organic solvent; removes caffeine; uses HPLC to separate the catechin, as epigallocatechin, etc. The inventive drug can be used to treat virus infection of respiratory tract.
EP1059940B1 topical compositions comprising an alpha 1-adrenergic blocker FOR TREATING PAINFUL CONDITIONS OF THE ANAL REGION Method and composition for treating painful conditions of the body and of the anorectal region. The compositions include a combination of nitroglycerin and sucralfate or a combination of nitroglycerin, lidocaine and sucralfate. The compositions also include a combination of an α-adrenergic blocker and sucralfate, a combination of α-adrenergic blocker and lidocaine, and a combination of an α-adrenergic blocker, lidocaine, and sucralfate. Alternatively, the composition may contain only an α-adrenergic blocker. Additional active ingredients for reduction of anal pain may be added to the composition, particularly capsaicin. The compositions may be included in a petrolatum base along with a water soluble lubricant. These compositions have been found effective in treating painful conditions in the anal region such as anal fissures, inflamed or recently thrombosed hemorrhoids, and chronic anal pain.
WO2009093208A3 Substituted 2-amino-3-sulfonyl-pyrazolo[1,5-a] pyrimidines/antagonists of serotonin 5-ht6 receptors, methods for the production and the use thereof The invention relates to novel substituted 2-amino 3-sulfonyl-pyrazolo[1,5-a] pyrimidines, to novel antagonists of serotonin 5-HT6 receptors, to novel medicinal substances, pharmaceutical compositions, medicinal preparations and to the methods for the production and and to a method for treating and preventing the development of different diseases of the CNS, the pathogenesis of which is caused by the disorder in monoaminergic signaling pathways, in particular by hyper- or hypoactivating serotonin 5-HT6 receptors. In general formula 1: Ar is optionally substituted aryl or optionally substituted heterocyclyl; R1 and R3, independently from each other, represent C1-C3 alkyl or phenyl; R2 is a hydrogen atom or C1-C3 alkyl; R4 1 and R4 2 independently from each other represent a hydrogen atom, optionally substituted C1-C3 alkyl or optionally substituted phenyl, or R4 1 and R4 2 together with a nitrogen atom, with which they are bonded, form optionally substituted heterocyclyl.
WO2007076473A3 Substituted pyrimidinyloxy ureas useful as inhibitors of protein kinases The present invention relates to compounds and methods useful as inhibitors of protein kinases, including B-Raf and several receptor tyrosine and cytoplasmic tyrosine kinases. The present invention is directed to new substituted pyrimidinyloxy urea compounds of Formulas II, III and IV and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulating of protein kinase activity in a human or animal subject are also provided for the treatment diseases such as cancers.
CN101002781A Tablets of vacyclovir hydrochloride, and its preparing method A tablet of valaciclovir hydrochloride is proportionally prepared from valaciclovir hydrochloride, microcrystalline cellulose, carboxymethyl starch sodium, magnesium stearate, etc. through mixing valaciclovir hydrochloride with microcrystalline cellulose, adding wetting agent, granulating, baking, adding others, tabletting and coating.
US7166641 Diclofenac salt of lidocaine The present invention provides pharmaceutically acceptable salts having local anesthetic and anti-inflammatory activities. The preferred pharmaceutically acceptable salt is a diclofenac salt of lidocaine. Diclofenac is a non-steroidal anti-inflammatory drug (“NSAID”). Lidocaine is a local anesthetic. Other NSAID (except the salicylic acid derivatives of NSAID) can be used to replace diclofenac and/or other local anesthetics can be used to replace lidocaine. The pharmaceutically acceptable salts are crystalline compounds, which are distinctively different from either the NSAID alone or the local anesthetic alone, as indicated by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), High Performance Liquid Chromatography (HPLC) and Fourier-Transformed Infrared Spectroscopy (FTIR) analyses. These pharmaceutically acceptable salts are suitable for use in topical treatment or parenteral injection to treat patients with localized pain, including muscle pain, joint pain, pain associated with herpes infection, and wound pain (such as surgical wound, burn wound etc.).
EP2219450A1 Alleviating neuropathic pain with eets and seh inhibitors The invention discloses methods of using cis-epoxyeicosantrienoic acids (EETs), inhibitors of soluble epoxide hydrolase (sEH), or a combination of an EET and an inhibitor of sEH, to alleviate neuropathic pain in subjects suffering from such pain.
US20120321602 Omega-3 fatty acid nutriceutical composition and optimization method A novel omega-3 fatty acid/lipid based nutraceutical composition and a method of optimizing said omega-3 fatty acid/lipid based nutraceutical composition. The nutraceutical composition and method is based on the insight that different forms of high omega-3 fatty acid lipids (e.g. triglyceride form, ethyl ester form, free fatty acid form, phospholipid form) have different molecular modes and levels of action. Specifically the phospholipid form is likely more effective at promoting membrane fluidity and permeability, while the free fatty acid form is likely more effective at regulating cell receptors, such as the PPARα receptors, that are responsible for various metabolic effects including lipid metabolism. The desirability of producing omega-3 compositions that may act synergistically and thus more robustly to improve health and to some extent mimic markers of life extension such as shown by caloric restriction, along with specific optimization methods, markers, and compositions are taught.
CN101928258A 1-(2-substituted phenylamino-4-methyl-thiazole-5)-3-substituted phenyl-acrylketone derivative, preparation method and pharmaceutical application thereof The invention relates to a 1-(2-substituted phenylamino-4-methyl-thiazole-5)-3-substituted phenyl-acrylketone derivative, a preparation method and pharmaceutical application thereof. The invention further relates to a medicinal composition of the derivative and pharmaceutically acceptable salt thereof and application of the derivative and the pharmaceutically acceptable salt thereof in preparing antineoplastic drugs. The derivative is prepared by performing condensation reaction on 2-substituted phenylamino-4-methyl-5-acetylthiazole thiazole and substituted benzaldehyde under the alkaline condition. The method has the advantages of easy acquirement of solvents, simple and controllable reaction condition, convenient after treatment and higher yield of target product.
EP2674166A1 Use of erythropoietin (EPO) for the local treatment of cancer treatment-associated osteo-necrosis of the jaw The present invention relates to the use of erythropoietin (EPO) for the local treatment of bisphosphonate-associated osteonecrosis of the jaw (BP-ONJ) in the context of a cancer therapy involving bisphosphonates, and other osteonecrosis, such as radioosteonecrosis.
CN101829061A Taxol nanoparticle composition and preparation method thereof The invention discloses a taxol nanoparticle composition and a preparation method thereof, belonging to the technical field of taxol preparations. The invention relates to taxol nanoparticle composition and nanosuspension, the high drug-loading taxol nanoparticle composition and nanosuspension is prepared by taking a surface stabilizer as a carrier, wherein the effective average particle size of the composition is less than 1000 nm; the suspension is subjected to freeze drying or spray drying to obtain the taxol nanoparticle preparation which can be intravenously injected or taken orally. The method of the invention is reliable, easy to operate and low in energy consumption, and avoids interference of organic solvent; meanwhile, the obtained taxol nanoparticle composition has higher bioactivity and can give full play to the curative effect of taxol.
CN1883666A Pharmaceutical composition for treating nephritis The invention discloses a pharmaceutical composition for treating nephritis wherein the raw material herbs include (by weight ratio) Chinese ephedra 1-15 parts, calcium sulphate 5-30 parts, yellow corktree bark 5-30 part, honeysuckle flower 5-30 parts, capsule of weeping forsythia 10-30 parts, aristolochia stem 1-20 parts, seed of Job's tears 30-50 parts, alisol 1-20 parts, polyporus umbellatus 1-20 parts, areca catecha 1-20 parts and cordate houttuynia 30-50 parts.
US20080139547 N-Hydroxyalkynylbenzamide (or hydroxamate) derivatives; anticarcinogenic and antiproliferative agents The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
EP2743275A1 Pharmaceutical composition containing honeysuckle extract and antibiotics, pharmaceutical kit, and use of honeysuckle extract for preparation of drug Provided is a pharmaceutical composition useful for prevention and/or treatment of diseases caused by bacteria, wherein the pharmaceutical composition comprising a honeysuckle extract containing iridoid compounds and an antibiotic. Also provided is a pharmaceutical kit comprising the honeysuckle extract containing the iridoid compounds and the antibiotics which are separately placed. The honeysuckle extract is used in combination with the antibiotics, the responsiveness of multi-drug resistant bacteria to antibiotics is improved, a clinical application prospect is presented, especially the current status of the refractory bacterial infection diseases caused by the pathogenic bacteria resistant to the antibiotics can be improved. Also provided is a use of the pharmaceutical composition and pharmaceutical kit in the preparation of drugs for prevention and/or treatment a diseases caused by bacteria. In addition, also provided is a use of the honeysuckle extract in the preparation of drugs for reversing bacterial resistance.
CN103349671A Resveratrol and spirulina composition and preparations and preparation method thereof The invention relates to a resveratrol and spirulina composition and preparations and a preparation method thereof. The composition comprises spirulina and high-purity resveratrol with the purity higher than 80%; the composition further comprises an astragalus root extract, a tartary buckwheat extract and vitamin C; and a solid preparation is prepared from the composition and adjuvants, wherein the adjuvants comprise hydroxymethyl cellulose, microcrystalline cellulose and beta-cyclodextrin, and the beta-cyclodextrin can be used for improving the solubility and stability of the composition and improving the bioavailability of the solid preparation. The solid preparation disclosed by the invention can be used for promoting the recovery of islet cells, improving glucose tolerance, lowering blood viscosity and the brittleness of capillaries, promoting blood circulation, lowering blood sugar and blood fat and protecting the liver, and has a very good treatment effect on the prevention or treatment of diabetes, complications of diabetes and cardio-cerebral vascular diseases.
WO2012002918A1 Formulation for osteoporosis The present invention relates to pharmaceutical formulations with high bioavailability comprising calcium, genistein and vitamin D in order to be used in the prophylaxis and treatment of osteoporosis and related diseases.
WO2010002970A3 Isolation of cyclopamine Provided are deglycosylation methods designed to optimize the yield of Veratrum alkaloid from Veratrum plant material and/or from an extract of Veratrum plant material.
US20120252749 Methods of Treating Cancer with Glut Inhibitors Methods of treating cancer comprising administering inhibitors of glucose transporters (GLUTs) are provided. Methods of predicting whether a cancer will respond to treatment with a GLUT inhibitor also are provided.
EP2661433A1 Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd) The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
US7261907 Administering to an animal subject in need thereof an effective amount of a composition comprising a clathrate of aliphatic material and monoclinic sulfur, wherein the aliphatic material is encapsulated by the monoclinic sulfur A non-stoichiometric clathrate of lipid and sulfur has been shown to effectively stabilize nerve cell membranes. As such, said compound has proven useful in a variety of neuropsychiatric disorders such as, addiction, depression, autism, Tourette's syndrome, and the like.
CN103459396A [1, 2, 4] triazolo [4, 3 -b] pyridazine compounds as inhibitors of c-met tyrosine kinase The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of the compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising the compound of the formula (I), optionally in the presence of a combination partner; and processes for the preparation of the compound of formula (I).
US20120277217 Imidazole Derivatives as IDO Inhibitors Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
WO2007070667A3 Crystal form of atorvastatin hemi-calcium and processes for preparation thereof Provided is a crystal form of atorvastatin hemi-calcium and processes for its preparation.
EP2181708A1 Use of Valproate for reducing CHOP levels, particularly in a mammal having SCI The present invention relates to the use of valproate in the manufacture of a drug for reducing CHOP levels in a mammal. In particular, said mammal has spinal cord injury (SCI), particularly traumatic SCI. The present invention, therefore, also relates to the use of valproate in the manufacture of a drug for treating SCI in a mammal, particularly traumatic SCI. The present invention also relates to a method for reducing CHOP levels in a mammal, particularly said mammal having spinal cord injury (SCI), specifically traumatic SCI. The present invention also relates to valproate for use in reducing CHOP levels in a mammal, particularly said mammal having spinal cord injury (SCI), specifically traumatic SCI.
WO2008105533A1 Adiponectin secretion-stimulating agent comprising capsinoid compound Disclosed is a substance which can increase the production and secretion of adiponectin when administered orally to a mammal and therefore can prevent or ameliorate metabolic syndrome in the mammal. Specifically disclosed is an adiponectin secretion-stimulating agent for a mammal, which comprises a capsinoid compound and/or a degradation product thereof as an active ingredient. The adiponectin secretion-stimulating agent can be used in an oral pharmaceutical composition for the treatment of a subject suffering from metabolic syndrome or a composition for preventing and/or ameliorating metabolic syndrome without causing the decrease in the body weight of a subject suffering from metabolic syndrome.
US20120014962 Method of inhibiting fibrogenesis and treating fibrotic disease The present invention relates to the discovery of an epigenetic relay pathway that controls hepatic stellate cell activation and the wound-healing response in fibrogenesis, including fibrogenesis of the injured liver. Methods of inhibiting fibrogenesis, including liver fibrogenesis and secondary disease states and conditions thereof, and in treating liver damage, including cirrhosis of the liver (which may be caused by viruses or chemicals, including alcohol), are aspects of the present invention. The methods utilize certain nucleoside compounds and/or antibodies which are optionally conjugated. Pharmaceutical compositions represent additional aspects of the invention.
CA2375787C Compositions and methods for increasing cholesterol efflux and raising hdl using atp binding cassette transporter protein abc1 The present invention relates to novel ABC1 polypeptides and nucleic acid molecules encoding the same. The invention also relates to recombinant vectors, host cells, and compositions comprising ABC1 polynucleotides, as well as to methods for producing ABC1 polypeptides. The invention also relates to antibodies that bind specifically to ABC1 polypeptides. In addition, the invention relates to methods for increasing cholesterol efflux as well as to methods for increasing ABC1 expression and activity.The present invention further relates to methods for identifying compounds that modulate the expression of ABC1 and methods for detecting the comparative level of ABC1 polypeptides and polynucleotides in a mammalian subject. The present invention also provides kits and compositions suitable for screening compounds to determine the ABC1 expression modulating activity of the compound, as well as kits and compositions suitable to determine whether a compound modulates ABC1-dependent cholesterol efflux.
WO2009077874A3 A pharmaceutical composition for treating esophageal cancer A compound represented by the following formula (I), a salt thereof or a hydrate of the foregoing is useful for treating esophageal cancer. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non- aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents -CH=, nitrogen or the like.]
CN102600071A Method for preparing sinomenine hydrochloride infusion solutions and freeze-dried powder injections The invention discloses a method for preparing sinomenine hydrochloride infusion solutions and freeze-dried powder injections. The method disclosed by the invention adopts adsorption technique of cation exchange resin or macroporous adsorption resin to replace traditional benzene extraction and chloroform extraction technique that are more toxic, and is high in extraction rate and simpler in operation; and harm and pollution to operators and the environment produced by the large-quantity high-toxicity organic solvent can be overcame, the method reduces processes for treating the organic solvent, is more beneficial for environmental protection, reduces investment in environmental protection facilities of plants, and is beneficial for environment-friendly production. Sinomenine hydrochloride extracted and separated by the method disclosed by the invention is used as a raw material in pharmaceutical preparations, has higher purity and no residual solvent, and reduces the potential hazards to human body.
WO2005061523A1 Glycosaminoglycan (gag) mimetics The invention relates to compounds that are designed to mimic the structure of GAGs; methods for the preparation of the compounds; compositions comprising the compounds; and use of the compounds and compositions thereof for the anti-angiogenic, anti-metastatic, anti-inflammatory, anticoagulant, antithrombotic, and/or antimicrobial treatment of a mammalian subject.
US20120190003 Organ arrest, protection, preservation and recovery The present invention relates to a composition for controlling viability of a tissue including a potassium channel opener or adenosine receptor agonist, a compound for inducing local anaesthesia and a compound for reducing the uptake of water by a cell in the tissue. The present invention also relates to the use of the composition according to the invention for controlling viability of a tissue.
US20110039893 Gsk-3beta inhibitor For the purpose of providing a GSK-3β inhibitor containing a 2-aminopyridine compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (IA): wherein each symbol is as defined in the specification. or a salt thereof or a prodrug thereof.
WO2008042806A3 Stilbenedisulfonic acid derivatives as inhibitors of retroviral integrase The present invention provides a class of novel stilbenedisulfonic acid derivatives. These compounds have the activity as inhibitors of retroviral integrase, an essential enzyme for the proliferation of retroviruses such as HIV-1. Also described in this application are pharmaceutical compositions comprising at least one of the stilbenedisulfonic acid derivatives and a method of using the stilbenedisulfonic acid derivatives to inhibit retroviral proliferation. In addition, this application provides a new method for identifying compounds that inhibits retrovirus integrase activity.
US20110124621 Benzothiazoles as ghrelin receptor modulators A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.
US20060147386 System and method for intranasal administration of lorazepam A therapeutic composition of lorazepam and its pharmaceutically acceptable derivatives are provided for intranasal administration of at least one predetermined volumetric unit dose in the form of a spray by means that delivers one or more therapeutically prescribed unit doses that are highly accurate as to the volume discharged and which leave no significant quantity of the composition in the delivery means.
US20110268785 Propynylaminoindan Transdermal Compositions Propynylaminoindan (e.g., Rasagiline) transdermal compositions are provided. Aspects of the transdermal compositions include a matrix of the propynylaminoindan in a pressure sensitive adhesive comprising a carboxylated polymer. In some instances, the matrix further includes a cationic acrylic copolymer. Also provided are methods of using the transdermal compositions and kits containing the transdermal compositions.
WO2008118879A2 Antiviral compositions comprising 2 compounds Described herein are compounds useful in the treatment of viral diseases, compositions comprising them and methods of using them. The compounds comprise a nucleoside or nucleoside analog linked, commonly through a phosphate group to one of a selected group of lipids. In some embodiments, the compounds described herein are useful for treating HIV infection, AIDS and other viral infections.
EP1498493A1 Method of examining allergic disease B1799 gene, whose expression level increases significantly in the patient group, was successfully identified by screening for a gene which shows difference in expression in blood collected from multiple healthy subjects and patients of allergic diseases employing the differential display method. The gene expression level is specifically high in T cells and increased due to T cell activation. This gene can be used in testing for allergic diseases and also in screening for therapeutic agents for allergic diseases.
CN101987149B External medicine for treating scrofula The invention relates to external medicine for treating scrofula, which has a raw material recipe comprising 1 to 5 parts of muskiness, 15 to 30 parts of centipede, 15 to 30 parts of scorpion, 15 to 30 parts of gecko, 20 to 100 parts of spurge, 20 to 100 parts of ranunculus sceleratus, 20 to 100 parts of taro and 5 to 100 parts of vinegar. The medicine is prepared by the following steps of: grinding the muskiness, the centipede, the scorpion and the gecko into powder; smashing the spurge, the ranunculus sceleratus and the taro to obtain juice; and finally, mixing the powder, the juice and thevinegar together. when in use, only a small amount of medicine is applied to affected part, the pain of patients from medicine taking, injection and operation can be relieved. In addition, the skin at the medicine application part can not be injured, and scars can not be left. The treatment time is short, and the curative effect can be fast realized.
CN102988304A Medicinal composition containing lysine hydrochloride compound The invention relates to a medicinal composition containing a lysine hydrochloride compound, and in particular relates to freeze-dried injection of lysine hydrochloride and a preparation method thereof. Each 1,000 injections are prepared from the following components: 3,000g of lysine hydrochloride, 100 to 200g of mannitol, 1 to 3g of ethylene diamine tetraacetic acid (EDTA) calcium, 1 to 2g of vitamin C, and 2,000ml of buffer solution of disodium hydrogen citrate and trisodium citrate in a mole ratio of 1:4.
EP1169059B1 Docetaxel in combination with rhumab her2 for the treatment of cancers The present invention relates to a method of treating cancer, comprising administering a dose of docetaxel and a dose of rhuMAb HER2 to a patient in need thereof, wherein said dosages have a synergistic therapeutic effect when compared to the administration of docetaxel or rhuMAb HER2 alone.
WO2012064286A1 Targeting metabolic enzymes in human cancer Targeting metabolic enzymes in human cancer Abstract Lung cancer is a devastating disease and a major therapeutic burden with poor prognosis. The functional heterogeneity of lung cancer (different tumor formation ability in bulk of tumor) is highly related with clinical chemoresistance and relapse. Here we find that, glycine dehydrogenase (GLDC), one of the metabolic enzyme involved in glycine metabolism, is overexpressed in various subtypes of human lung cancer and possibly several other types of cancers. GLDC was found to be highly expressed in tumor-initiating subpopulation of human lung cancer cells compared with non-tumorigenic subpopulation. By array studies we showed that normal lung cells express low levels of GLDC compared to xenograft and primary tumor. Functional studies showed that RNAi inhibition of GLDC inhibits significantly the clonal growth of tumor-initiating cells in vitro and tumor formation in immunodeficient mice. Overexpression of GLDC in non-tumorigenic subpopulation convert the cells to become tumorigenic. Furthermore, overexpression of GLDC in NIH/3T3 cells and human primary lung fibroblasts can transform these cells, displaying anchorage-independent growth in soft agar and tumor-forming in mice. Not only is GLDC is expressed human lung cancer, it is also up-regulated in other types of cancer, such as colon cancer. RNAi knockdown of GLDC in colon cancer cell line, CACO-2 cells, can also inhibit the tumor formation in mice. Thus GLDC maybe a new metabolic target for treatment of lung cancer, and other cancers.
CN101317835A Application of cantharidin and its derivant in preparing sensitization medicament for tumour chemotherapy The present invention discloses purpose of cantharidin and derivative in preparation of tumour chemotherapy hypersensitivity medicine, which is used for enhancing the sensibility of tumour on the therapeutic drug. The compound and the derivatives to which he present invention relates have the functions of decreasing MDR genetic transcriptiion and expression in various tumor cells and further restraining the occurrence of multi-drug resistance and shows stronger tumour chemotherapy hypersensitivity function.
US8173805 sEH inhibitors and their use The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R4, R5, R6, A, B, Y, Z, n, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
CN103209997A High purity heparin and production method therefor The present invention provides a high purity heparin useful as a medicine, a cosmetic, a research reagent and the like, and a production method therefor, in more detail, a method for producing heparin, the method comprising mixing a heparin without substantially containing nitrous acid degradation-resistant impurities with 0.2 to 1 time (volume) the amount of ethanol to 5 to 30 wt% of heparin solution, and obtaining a colloidal precipitate of heparin.
EP0602112B1 High content ibuprofen agglomerates and process to prepare them A process for the preparation of a pharmaceutical composition in the form of agglomerates comprising 70-97 % by weight of 2-(4-isobutylphenyl)propionic acid or a pharmaceutically acceptable salt thereof and 3-30 % by weight of a starch component, said process comprising the steps of a) forming an emulsion comprising 1) 70-97 % by weight of 2-(4-isobutylphenyl)propionic acid or a salt thereof; 2) a solvent system; 3) 3-30 % by weight of the starch component; 4) water and optionally 5) a surfactant; b) crystallising to produce a suspension comprising crystals of 2-(4-isobutylphenyl)propionic acid or the salt thereof in intimate contact with the starch component; c) agitating said suspension to form agglomerates comprising an evenly distributed mixture of 2-(4-isobutylphenyl)propionic acid or a salt thereof and the starch component; d) collecting said agglomerates and optionally e) drying said agglomerates. Pharmaceutical formulations comprising 90-99.98 % by weight of such a composition together with 0.02-10 % of a pharmaceutically acceptable excipient are also described, which are suitable for direct compression into tablets. Preferably the starch component comprises a mixture of maize starch and pregelled maize starch.
CN103156855A Paracetamol and caffeine slow-release capsule and preparation method thereof The invention discloses a paracetamol and caffeine slow-release capsule and a preparation method thereof. The paracetamol and caffeine slow-release capsule is prepared by filling paracetamol and caffeine slow-release micropills into a capsule. The preparation method comprises the following steps: coating a medicated layer and a coating layer on the blank pill cores to obtain paracetamol and caffeine slow-release micropills, and filling the paracetamol and caffeine slow-release micropills into the capsule. The medicine disclosed by the invention has the advantage of uniform release, can achieve the goal of persistent effect and higher curative effect, and can lower the dosage on the premise of maintaining identical drug effect, thereby reducing the side effect on the patient due to lower dosage of the medicine; and the preparation technique is simple, has the advantage of stable product quality, and is applicable to large-scale production.
CN101342144A Acetaminopher DC90 fine particle and preparation method thereof The invention discloses paracetanol DC90 fine particles and a preparation method thereof. The paracetanol DC90 comprises following materials by weight ratio: 90 percent of paracetanol, 3.50 percent of cornstarch, 3.50 percent of pre gelatinized starch, 2.00 percent of povidone, 0.5 percent of crospovidone and 0.5 percent of stearic acid. Firstly, the paracetanol and the cornstarch are mixed evenly, then the pre gelatinized starch and the povidone are made into starch slurry to be used as bond which is evenly sprayed on the mixture of the fluidied paracetanol and cornstarch, fluidized bed granulation is carried out in the inlet air temperature, the wet particles are dried under the temperature of 80 DEG C and then are cooled at the temperature of 50 DEG C till water conforms to the requirement, the sizes of the particles are adjusted, the stearic acid and the crospovidone are added after the particle sizes are adjusted to be mixed evenly to obtain the paracetanol DC90 fine particles. The invention adopts the above technical proposal to inspect the product, and the particles are fine and uniform and have favorable fluidity, thereby being well and evenly mixed with other small quantities of active components powder.
WO2008128685A1 Use of a composition comprising formoterol and beclometasone dipropionate for the prevention and/or treatment of an exacerbation of asthma The present invention relates to the use of a composition comprising a fixed combination of a) formoterol, a pharmaceutically acceptable salt or solvate thereof or a solvate of such a salt; and b) beclometasone dipropionate; for the manufacture of a medicament for use in the prevention and/or treatment of an exacerbation of asthma, intermittent asthma and/or episodes in chronic asthma during the maintenance therapy of asthma with the same composition for symptomatic relief, when needed.
WO2013161359A1 Enteral environment-improving agent An enteral environment-improving agent comprising a starch that has a high resistant starch content and fulfills the requirements (a), (b), (c) and (d) mentioned below as an active ingredient: (a) the resistant starch content is 60% or more as measured by a resistant starch measurement method in accordance with the AOAC official method 2002.02;(b) the molecular weight peak is 6 × 103 to 4 × 104 inclusive; (c) the molecular weight dispersion degree is 1.5 to 6.0 inclusive; and (d) the enthalpy of gelatinization at 50 to 130˚C is 10 J/g or less as measured by differential scanning calorimetry.
CN102688237A Stable Azelnidipine composition Azelnidipine is a dihydropyridine calcium channel blocker and is widely used due to reliable antihypertensive effect. Azelnidipine is characterized by long duration of effect and mild effect. In the preparation of a Azelnidipine composition, incompatibility will cause decreasement of content of main drug of composition and increasement of content of a related substance. Azelnidipine and ethyl cellulose are comprised according to the technical scheme provided by the invention. The technical scheme is characterized in that Azelnidipine is coated by an ethanol solution of ethyl cellulose with a certain concentration and then subjected to granulating and tableting to obtain a stable composition.
WO2012006104A3 Compounds and methods for treating tuberculosis infection The present invention provides compounds which are potent inhibitors against Lpd activity, PDH activity, and/or the growth of tubercle bacillus, and thus are useful in the treatment of tuberculosis infection and associated conditions. The present invention is further directed to in vitro- and in vzivo-based methods of inhibiting Lpd and/or PDH activity. In certain embodiments, these methods are useful in inhibiting Lpd and/or PDH activity key to a pathogen' s survival.
CN102796078A Pantoprazole compound, preparation methods and pharmaceutical preparations thereof The invention belongs to the technical field of pharmaceutical compounds, and relates to a pantoprazole sodium compound entity, especially a pantoprazole sodium crystal form, preparation methods and pharmaceutical preparations thereof. The pantoprazole sodium compound is crystal, and measured by X-diffraction powder diffraction, and the diffraction pattern has the following diffraction angles (2Theta) in turn: 9.5 degrees, 10.4 degrees, 11.6 degrees, 13.1 degrees, 13.8 degrees, 14.2 degrees, 15.0 degrees, 15.3 degrees, 15.9 degrees, 16.5 degrees, 17.5 degrees, 18.0 degrees and 18.2 degrees. The pantoprazole sodium compound entity may be associated with a variety of lyophilization supporting agents and the prepared lyophilized powder for injection has good solubility, good clarity and low content of related substances, etc. simultaneously the use level of the used lyophilization supporting agent is relatively less, the cost of the products is reduced, and the stability and quality of the products are improved.
CN101524531A Preparation and application of pharmaceutical composition containing collagen and isosorbide mononitrate The invention discloses a pharmaceutical composition for treating impotence and frigidity. Penis cavernous tissue of an impotence patient has obvious pathological changes, and the pathological damages are possibly related to ischemia and hypoxia in local tissues and lack of collagen. Therefore, local application of small molecular collagen absorbed through skin is helpful for improving the toughness of penile tissues as well as the elasticity and the tensility of the tissues; the main pharmacological actions of isosorbide mononitrate include relaxing smooth muscles and expanding peripheral blood vessels, and local application can ensure cavernous hyperaemia and penile erection; combined local application of collagen and isosorbide mononitrate only requires small doses and almost has no side effects of oral drugs; isosorbide mononitrate does not arouse sexual desire and just assists a patient in restoring normal erection function when sexual excitement appears; moreover, the drug composition also has remarkable curative effects of improving female frigidity, thereby providing a novel choice for treating the impotence and the frigidity.
US7939504 Method of treating skin ulcers with vectors encoding hepatocyte growth factor The present invention relates to a therapeutic preventive agent that includes an angiogenic factor gene (such as hepatocyte growth factor (HGF), vascular endothelial growth factor (VEGF), fibroblast growth f actor (FGF), and hypoxia inducible factor (HIF)) as its active ingredient, and the administration of such an agent into the targeted skin diseases-affected area.
WO2006113571A3 Substituted cyclopentanones for treating inflammatory bowel disease Compounds are disclosed herein comprising formula (I) or a pharmaceutically acceptable salt, or a metabolite or a prodrug thereof; wherein a dashed line indicates the presence or absence of a bond; Y, A, and B are described herein. Therapeutic uses, manufacturing methods, compositions, and medicaments related thereto are also disclosed.
CN102813647A New compound separated and identified from usnea longissima fruticose thallus The invention relates to a new natural compound separated from usnea longissima, which is 2-Benzofuranbutanoic acid, 7-acetyl-C-[(7-acetyl-2, 3-dihydro-4,6-dihydroxy-3,5-dimethyl-2-oxo)-3-benzofuranyl]-4,6-dihydroxy-3,5-dimethyl-B-oxo-, ethyl ester. The compound has potential antibacterial activity and the like; the invention also provides a preparation method of the compound; the research indicates that the compound has a spatial isomer and the two coexist or change mutually; and the special structure has a functional group with antibacterial activity and the like. The research belongs to the extraction and preparation of the active ingredients of crude medicines and the application method thereof in the field of medicine and health care products, and provides a basis for developing a new medicine and a new medicine primer.
EP1610797A1 Antiviral combination of nevirapine and a further antiretroviral compound In accordance with the present invention there is provided a pharmaceutical composition useful for the treatment or prophylaxis of viral infections comprising nevirapine and at least one antiviral active compound of formula (I), wherein Base is selected from the group consisting of thymine, cytosine, adenine, guanine, inosine, uracil, 5-ethyluracil and 2,6-diaminopurine, or a pharmaceutically acceptable salt or prodrug thereof, an example of such antiviral active compound being alovudine.
EP2145897A2 Therapeutic methods and compositions based on serrate proteins and nucleic acids The present invention relates to pharmaceutical compositions comprising a fragment of Serrate protein or a derivative or analog of said fragment, or comprising a derivative or analog of a Serrate protein, or comprising a protein comprising such a fragment, derivative or analog, the fragments, derivatives, analogs and proteins being characterized by the ability in vitro, when expressed on the surface of a first cell, to bind to a Notch protein expressed on the surface of a second cell. The invention also relates to chimeric proteins comprising said Serrate fragments joined via a peptide bond to a protein sequence of a protein different from the Serrate protein, and to nucleic acids encoding said fragments of a Serrate protein, and encoding said chimeric proteins. According to the invention, said fragments, derivatives, analogs, and proteins, said chimeric proteins and said nucleic acids may be used as a medicament, for example, in treating or preventing malignancy in a subject.
US7563586 Tetrodotoxin resistant membrane protein for use in pain management The present invention provides a method of identifying a modulator of a voltage gated sodium channel (VGSC), which method comprises bringing into contact a VGSC, a p11 peptide and a test compound under conditions where the VGSC and the p11 peptide are capable of forming a complex in the absence of the test compound; and measuring an activity of the VGSC, wherein a change in the activity of the VGSC relative to the activity in the absence of the test compound indicates that the test compound is a modulator of said VGSC. Compounds identified in such screening methods are proposed for use in the treatment of VGSC-related conditions, for example in the treatment or prevention of pain. Also provided are methods of enhancing the functional expression of a voltage gated sodium channel (VGSC) in a cell comprising the step of increasing the level of p11 in the cell.
WO2014091298A3 Nitrogen containing morphinan derivatives and the use thereof The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1-R4, Y, and Z are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I) to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
CN103342759A Novel biological material with controlled release of nitrogen monoxide under catalysis of enzyme, as well as preparation method and application thereof The invention discloses a novel biological material with controlled release of nitrogen monoxide under catalysis of an enzyme, as well as a preparation method and application thereof. The novel biological material with the controlled release of the nitrogen monoxide under the catalysis of the enzyme is prepared by connecting a nitrogen monoxide donor compound with stable glycosylation with a natural polymer, namely chitosan through covalent bonds. The material has good processability and can be prepared into injectable solutions, thin films, porous supports, electrostatic spinning fiber films and other various products. The CS-NO and a composite material thereof can be used for treating diabetic lower limb ischemia, skin injures and myocardial infarction disease. As the nitrogen monoxide can be released in a controlled manner according to requirements, the material shows a great effect in treatment.
CN101485637B Colchicine framework controlled release tablets or capsules The invention discloses a colchicine framework controlled-release tablet or capsule, which comprises colchicines and framework materials having controlled-release function, wherein the framework materials contain hydrophilic polymers of which the weight against the weight of the tablet is at least 20 percent and other pharmaceutic adjuvants; and the tablet or capsule comprises the following components in percentage by weight: 0.01 to 1.0 percent of colchicine, 20 to 85 percent of hydrophilic polymer, 1 to 30 percent of retarder, 20 to 60 percent of bulking agent, and 0.1 to 2 percent of lubricant. Release degree test results show that more than 90 percent of drugs are continuously released in vitro in 12 hours; and compared with the common tablet, the tablet or capsule has the advantages of obviously reducing daily taking frequency, lowering toxic and side effects of the drugs and improving the compliance and curative effect of patients.
US6962919 Gonadotropin-releasing hormone antagonizing activity; useful as prophylactic or therapeutic agent for sex hormone-dependent diseases A compound of the formula: wherein one of A and D is N and the other is C, or both are N; B is N or C; m is 0-3; R1, R2 and R3 each is (i) H or (ii) a group bound via C, N, O or S; R4 is a group bound via C; R5 is H or a group bound via C or O; R6 is H or a group bound via C; R7 is a homo- or hetero-cyclic group which may be substituted; or a salt thereof possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful as a prophylactic or therapeutic agent for sex hormone-dependent diseases, and so forth.
WO2009097306A1 Substituted pyridazine derivatives which have histamine h3 antagonist activity The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.
US20110217280 Methods for treating neuropsychiatric conditions Provided herein are methods for treating a subject suffering from a neuropsychiatric condition (e.g., schizophrenia). The methods include systemic administration of a pharmacological composition containing a therapeutically effective amount of a PAK activator.
WO2010118347A2 O-linked glycan biosynthesis modulators Provided herein are O-linked glycan inhibitors, including modulators of polypeptide GalNAc transferase, core transferase, polylactosamine-modifying glycosyl transferase, polylactosamine extension enzyme, core 1 specific chaperone, sialyl transferase, fucosyl transferase, and O-linked glycan sulfotransferases.
CN102126999A Catalytic synthesis method of chiral azetidin-2-one-4-amide and carboxylic acid compounds in microorganism system The invention discloses a catalytic synthesis method of chiral azetidin-2-one-4-amide and carboxylic acid compounds in a microorganism system. The structural general formulas of the chiral compounds are shown in the formula I and the formula II. The preparation method is that racemic azetidin-2-one-4-nitrile or amide compounds performs catalytic hydrolysis in a Rhodococcuserythropolis AJ270 microorganism system to obtain the target products. The dosage of Rhodococcuserythropolis can be adjusted according to the dosage of the substrate. The reaction solvent is common buffer solution of which pH value is 6.0-8.0, the temperature is 20-37 DEG C and the reaction time is from 3 hours to 8 days. The method is characterized in that the method has the advantages of efficient reaction, mild reaction conditions and high enantioselectivity, and is simple in operations, and the product is easy to separate and has high product; and the method has good application prospect.
US20110236371 Compositions And Methods For The Treatment Of Neurologic And Psychiatric Conditions The invention provides pharmaceutical compositions and methods of use thereof for preventing or ameliorating disorders of the nervous system. More specifically, the invention provides pharmaceutical compositions, including phosphopeptides, that when administered disrupt TrkB-mediated activation of PLCγ1 phosphorylation. The invention further provides method of treatment comprising administering inhibitors of TrkB-mediated activation of PLCγ1 phosphorylation alone or in combination with other pharmaceutical compositions to prevent or ameliorate nervous system disorders such as epilepsy, stroke, anxiety, migraine, and pain.
US20100178325 Amphiphilic nucleotide cochleate compositions and methods of using the same The present invention is directed to cochleate compositions that include a nucleotide that is associated with a positively charged amphiphile. The present invention also includes methods for making and using the compositions provided herein.
EP2143433A1 Preparation for the prevention of joint disease According to this invention, the above-mentioned disadvantages are removed by the product for prevention of joint disease, the basis of which is the content of 10 to 1,000 mg of hyaluronic acid and/or salts from it in 100 to 1,000 grams of the medicine's carrier. The advantage of the product for the prevention of joint diseases is that it has an instant ingredient or sugar in the carrier. The advantage of the product for the prevention of joint diseases is that the carrier is formed by a liquid. The advantage of the product for the prevention of joint diseases is that it contains a mixture in the carrier for the production of snack sticks.
EP1583538A1 Use of 3-methoxy-pregnenolone in the production of a medicament for treating neurodegenerative diseases The invention relates to a novel use of derivatives of neurosteroids, particularly pregnenolone, for the treatment of acute or chronic lesions of the nervous system, especially certain neurodegenerative diseases, related in particular to the ability thereof to stabilize and/or increase the polymerization of neuronal microtubules.
US7915281 Isoxazole, dihydroisoxazole, and oxadiazole substituted imidazo ring compounds and method Imidazo ring compounds, (e.g. imidazo[4,5-c]pyridine, imidazo[4,5-c]quinoline, 6,7,8,9-tetrahydro imidazo[4,5-c]quinoline, and imidazo[4,5-c]naphthyridine compounds) having an isoxazole, dihydroisoxazole, or oxadiazole substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
WO2014147204A1 Heteroaryl substituted indazoles Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
CN103242231A Quinoline derivatives as well as preparation methods and applications thereof The invention relates to novel substituted quinoline derivatives shown as the general formula I and medicinal acid addition salts of the novel substituted quinoline derivatives. The compounds provided by the invention are specially defined as the specification, wherein R1 and R2 are respectively independent methyl, ethyl or benzyl, or R1 and R2 and N connected with R1 and R2 can form 4-methyl-piperidyl or morpholinyl, and n=1 or 2. The invention also relates to preparation methods of the compounds provided by the invention. Pharmacological activity screening tests show that the compounds have remarkable hyperplasia preventing effects for cancer cells in vivo and in vitro, and parts of compounds have remarkable tumor suppression activity, such as lung cancer, liver cancer, breast cancer and pancreatic cancer. Particularly, the tumor inhibiting rate of the pancreatic cancer PANC (Pancreatic Cancer Cell)-1 is up to 46.7%.
CN101205231A Tetrahydroisoquinoline derivatives having multi-medicine resistance regulation activity and synthesis thereof The invention discloses a tetrahydroisoquinoline derivative with the MDR activity, which comprises one of the compounds 2a, 2b, 2c, 2d, 2e, 2f, 2g, 2h, 2i and 2j. The tetrahydroisoquinoline derivative is constructed through the smile rearrangement reaction in the mode of applying the one-pot method to the N-substituted-2-chloroacetamides and 2-bromine-3-hydroxypyridine and then is obtained through the Pictet-Spengler cyclization. The yield of the final target products ranges from 17 per cent to 37 per cent; the change of the substituent (R) and the compounds show better MDR reversal activity.
CN103417500A Cobamamide freeze-drying agent and preparation method thereof The invention relates to a cobamamide freeze-drying agent and a preparation method thereof. A proportion of cobamamide, dextran 40, mannitol, sodium chloride and water for injection is 1g:10g:10-30g:10-30g:1000ml. The preparation method includes the following steps: 1), weighing the dextran 40 according to the proportion, dissolving, adding prescribed amount of sodium chloride and mannitol, stirring for dissolving, adding the water for injection to 90% of total amount, adding activated carbon and stirring, roughly filtering to remove carbon, and adding water to the total amount; 2), after cooling, weighing prescribed amount of cobamamide, adding the cobamamide into a proppant solution after carbon removal, dissolving prior to filtering for degerming by using a 0.22um microhole filtering film; 3), sub-packaging; 4), freeze-drying; 5), pressing a cover in a box, and taking out a sample after restoring to normal pressure. The preparation method is simple in operation, needless of protection from light and protection of inertia gas and high in product stability.
US20110224238 6, 9-Disubstituted Purine Derivatives and Their Use for Treating Skin The present invention provides methods and compositions for countering the adverse effects of aging on mammalian cells in vitro and in vivo, especially human skin cells and human skin, and treatment of hyperproliferative and related skin diseases in mammals by administering compositions containing 6,9-disubstituted purine derivatives.
US6992080 For therapy of cancer, inflammation, arthritis, viral diseases, neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, and fungal diseases In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyridine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
CA2610881A1 Eye drop containing roflumilast An object of the invention is to enhance the efficacy of roflumilast in an eye drop containing roflumilast as an active ingredient. By blending at least one type of thickening agent in the eye drop containing roflumilast as an active ingredient, an eye drop in which the efficacy of roflumilast is enhanced can be prepared.
CA2392453C Modulation of signal transduction A polypeptide is identified as being functionally included in a signal transduction pathway having a biological effect. Contemplated polypeptides are different from a retinoic acid receptor, a retinoid X receptor, or a cellular retinoic acid binding protein, however, binding of the retinoid or retinoid metabolite lead to a modulation of the biological effect. In particularly contemplated methods, a retinoid or retinoid metabolite is administered to a cell or mammal in a concentration effective to modulate the biological effect.
CN102309496A Pharmaceutical composition for treating cardiovascular and cerebrovascular diseases The invention relates to a pharmaceutical composition for treating cardiovascular and cerebrovascular diseases and an application. The pharmaceutical composition takes ginsenoside Rd and luteolin as main components, is capable of obviously minimizing an infarction area of brain tissue and obviously mitigating the behavior obstacle due to necrotic brain tissue, and achieves the purpose of treating insufficiency of cerebral blood supply, cerebral thrombus, brain embolism, cerebrovascular spasm, brain dysfunction, Alzheimer disease, parkinsons syndrome, cerebral apoplexy, hypertension, hyperlipoidemia, arteriosclerosis, coronary heart disease, angina pectoris and miocardial infarction.
CN101716159B Stable lansoprazole tablet and preparation method thereof The invention discloses a stable lansoprazole tablet. The tablet comprises a tablet core, an isolated coat layer and an enteric coat layer, wherein the tablet core consists of lansoprazole, lactose, pregelatinized starch, croscarmellose sodium, lauryl sodium sulfate and magnesium stearate; the isolated coat layer is made from Opadry Y-1-7000, ethanol and purified water; and the enteric coat layeris made from Opadry OY-P91 S-type and ethanol. In addition, the invention also discloses a preparation method of the lansoprazole tablet. Through the bioavailability test, the stability test and the stability contrast test of a human body, the lansoprazole tablet of the invention is proven to have high bioavailability and stable quality.
CA2350560C Novel type condensed pyridazinone compounds Novel pyridazino[4,5-b][1,5]oxazepinone thiazepinone and diazepinone derivatives of general formula (I) wherein: R stands for hydrogen atom or a group of formula NHR4 wherein: R4 stands for hydrogen, C1-4 alkyl or C2-5 acyl group, R1 stands for C1-4 alkyl or C2-4 alkenyl group, which may be substituted by a phenyl group, or phenyl group, W stands for methylene or carbonyl group, X and Ystand independently for oxygen or sulphur atom, SO, SO2 or NR3 group, wherein R3 is hydrogen atom, C1-4 alkyl group or a group of formula (II), wherein R2 stands for hydrogen or halogen atom, C1-4 alkoxy or nitro group or a group of formula NHR4, wherein R4 has the above meaning, and Z stands for methylene or carbonyl group, further n has a value of 0, 1 or 2 with the proviso that when any of X or Y stands for oxygen or sulphur atom, SO or SO2 group or a group of formula NR3, wherein R3 stands for hydrogen atom or C1-4 alkyl group, then the other may stand only for an NR3 group, wherein R3 stands for a group of formula (II) - wherein R2, Z and n have the above meanings - and their tautomers and the acid-addition salts of all these compounds. The compounds according to the invention show memory-enhancing and neuroprotective properties.
US20100310543 Method of preventing and treating acute brain pathologies Described are novel means in the treatment of cerebral neurological conditions such as ischemic insult of the brain. Furthermore, a kit for a non-radioactive protein serine/threonine phosphatase activity assay is provided, which is capable of detecting and distinguishing the activity of PP1, PP2A, and calcineurin (PP2B).
US7625908 Antiproliferative agent in the prevention or treatment of tumors which are sensitive to inhibition of EGF and erbB receptor tyrosine kinases;1-({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)-L-prolinamide A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.
EP2252605A2 Labelled analogues of halobenzamides as multimodal radiopharmaceuticals and their precursors The present invention relates to the compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1 -C4 )alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1 -C4 )alkyl group or forms together with the group R1 -Ar a ring fused with the Ar group, A represents a group of formula (β) or (δ): R3 and R4 independently represent a hydrogen atom, a (C1 -C6 )alkyl group, a (C1 -C6 )alkenyl group or a group of formula (y): wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a -NO2 group, a -NR5 R6 group, a N+R5R6R7X- group, or a -OSO2R12 group, and their addition salts with pharmaceutically acceptable acids. The present invention also relates to pharmaceutical compositions comprising themand to their use in diagnosis, in particular with SPECTor PET imaging and in therapyofmelanoma, viatargeted radionuclide therapy.
CN102526068A Medicinal composition for treating female postmenopausal osteoporosis The invention belongs to the technical field of medicines, and discloses a medicinal composition for treating female postmenopausal osteoporosis. The medicinal composition consists of estradiol, levonorgestrel and pharmaceutic adjuvants, wherein the pharmaceutic adjuvants comprise a filling agent, a disintegrating agent, a bonding agent, a cosolvent and a lubricating agent; the grain diameter of the estradiol is 10 to 30 micrometers, the grain diameter of the levonorgestrel is 3 to 10 micrometers, the grain diameter of the filling agent is 140 to 160 micrometers, the grain diameter of disintegrating agent is 140 to 160 micrometers, and the grain diameter of the cosolvent is 140 to 160 micrometers. According to the medicinal composition, the grain diameters of the raw materials and the adjuvants are determined through experiments by taking content uniformity and dissolution as indexes; and experimental results indicate that the preparation of the medicinal composition is high in quality.
US20090012075 Fluorinated Arylamide Derivatives The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.
US20120316111 BMP-2 Upregulating Compounds For Healing Bone Tissue And Screening Methods For Selecting Such Compounds The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of one or more of the following compounds prazosin, quinacrine, emetine, apomorphine, and debrisoquine, whereby endogenous BMP-2 up-regulation is stimulated in said subject. The endogenous BMP-2 up-regulation may enhance bone formation and/or cartilage formation.
US7750037 Antidepressant A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X: O or S; Y: O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.
US20090233957 (-)-beloxepin and methods for its synthesis and use This present disclosure provides compositions comprising (−)-beloxepin, methods for their synthesis and methods for their use.
CN101579307A Application of hypertonic injection to preparation of medicament accelerating wound healing The invention relates to the application of hypertonic injection to the preparation of medicament accelerating wound healing. The hypertonic sodium chloride hydroxyethyl starch 40 injection, the hypertonic sodium chloride dextran 70 injection or the hypertonic sodium chloride hydroxyethyl starch 200/0.5 injection is preferentially used. The medicament is used for accelerating the healing of scratch, contusion, puncture, burn, incision, operation, frostbite, bite wound or wound caused by acidic material, alkaline material or corrosive material particularly in the perioperative period as the injection.
EP1019372B1 Fused pyrrolecarboxamides; a new class of gaba brain receptor ligands The present invention encompasses structures of formula (I) or the pharmaceutically acceptable non-toxic salts thereof wherein G represents (1) where Q is aryl substituents optionally mono or disubstituted with hydroxy or halogen; T is halogen, hydrogen, hydroxyl, amino or alkoxy having 1-6 carbon atoms; W is oxygen, nitrogen, sulfur, or optionally substituted methylene; X is hydrogen, hydroxyl, or alkyl; Z is an organic or inorganic substituent optionally forming a ring with substituents on Q; (2), (3) and (4) independently represent optionally substituted carbon chains; wherein k, m, and n are independently 0, or an integer of from 1-3; R3, R4, R5, and R6 are the same or different and represent organic or inorganic substituents. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
WO2005023231A1 Polypyrimidine tract binding protein promotes insulin secretory granule biogenesis The present invention relates to a method for stimulating production of secretory granules in peptide hormone-secreting endocrine cells or neurons comprising the step of promoting the presence of polypyrimidine tract binding protein (PTB) or a biologically active fragment or derivative thereof in the cytoplasm of said cells or neurons. Preferably, the method alternatively or further comprises promoting the activity of PTB or said biologically active fragment or derivative thereof in the cytoplasm of said cells or neurons. It is also preferred that said promotion comprises the promotion of the nucleocytoplasmic transport of PTB. In another aspect, the invention relates to a method of screening for an agent capable of stimulating production of secretory granules in peptide hormone-secreting endocrine cells or neurons comprising the steps of (a) contacting a cell capable of forming secretory granules and expressing polypyrimidine tract binding protein (PTB) or a biologically active fragment or derivative thereof with one or more compounds; and (b) assessing whether said one or more compounds promote the presence or activity of said polypyrimidine tract binding protein (PTB) or said biologically active fragment or derivative thereof in the cytoplasm of said cell. Comprised by the invention are further methods of screening for an agent useful as a cure for diabetes, sleeping disorders or depression as well as various medical uses of an agent capable of the promotion/reduction of the presence or activity of polypyrimidine tract binding protein (PTB) or of a biologically active fragment or derivative thereof. In alternative embodiments, the reduction or downregulation of PTB or said biologically active fragment or derivative thereof is considered.
WO2013083070A1 1, 4-dihydro-naphthyridine derivative and pharmaceutical composition and use thereof Disclosed are 1, 4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1, 4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia.
US20070021460 5-HT7 antagonists; irritable bowel syndrome; diarrhea, constipation The present invention provides a piperidine derivative represented by the following formula or analogs thereto, which are used for agents for treating or preventing various diseases related to 5-HT7.
WO2011053801A3 Methods and cosmetic preparations for the sustained delivery of therapeutic agents to the eye Cosmetic compositions comprising therapeutic agents for the treatment of various eye conditions and methods of use are described. In particular, the invention provides cosmetic compositions comprising ophthalmic therapeutic agents in combination with a muscle fasciculating agent for application to the outer surface of the upper eyelid, perimeter of the eyelid and/or eyelashes thereby causing transfer of the therapeutic agents into the vascular network within the eyelid for delivery into all parts of the eye, including the posterior segments of the eye, the eyelid glands, conjunctiva and periocular tissue.
US20080032970 Amide Derivatives of 7-Amino-3-Phenyl-Dihydropyrimido[4,5-D]Pyrimidinones, Their Manufacture and Use as Pharmaceutical Agents The present invention relates to novel amide derivatives of 7-amino-3-phenyl dihydropyrimido[4,5-d]pyrimidinones, to a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. The present derivatives are new compounds of the general formula (I).
US20120315256 Use of transforming growth factor - beta 1 (tgf-b1) inhibitor peptides for the treatment of corneal fibrosis and/or haze The invention refers to the use of transforming growth factor-beta 1 (TGF-β1) inhibitor peptides or polynucleotides encoding said peptides for the prevention and/or treatment of corneal fibrosis and/or corneal haze.
US7625579 A substrate having a vapor deposited furanone compounds, covalent bonding through etherification or amination; protective coatings on medical equipment, seeds, fibrics, wool, hair, silk, cotton, chitin, collagen, animal The present invention provides a substrate having a plurality of immobilised furanone moieties associated with at least part of a surface of the substrate. The invention also relates to articles consisting of or comprising such a substrate.
WO2009043958A1 Use of atomic quantum clusters (aqc) as antimicrobial agents and biocides The invention relates to the use of stable atomic quantum clusters (AQC) with antimicrobial activity. The stable AQCs include at least 500 metal atoms (Mn, n<500), the metals being selected from among Au, Ag, Co, Cu, Pt, Fe, Cr, Pd, Ni, Rh, Pb or bi- or multi-metallic combinations thereof. Said AQCs are used as antimicrobial agents, antifungal agents and biocides at concentrations of the order of between 1 nM and 100 nM or more in relation to atoms of the corresponding metal. The antimicrobial activity is specific to both the type of metal and size of cluster used.
CN102302618A Summer-heat relieving agent The invention discloses a summer-heat relieving agent. The summer-heat relieving agent comprises, by mass, 10-15 parts of quercus jenseniana hand-mazz, 10-20 parts of gomphrena globosa, 10-20 parts of negundo chastetree leaf, 10-15 parts of of plantain, 10-15 parts of Jisu powder and 10-20 parts of medlar. The summer-heat relieving agent further comprises, by mass, 5-10 parts of self-heal and 5-10 parts of the Jisu powder. According to the present invention, the quercus jenseniana hand-mazz, the gomphrena globosa, the negundo chastetree leaf, the plantain, the Jisu powder, the medlar, the self-heal, the Jisu powder and other pure natural plants are added to the summer-heat relieving agent, wherein the Jisu powder can be provided for treating common cold and wind cold, and can provide effects of summer-heat relieving, heat clearing and dampness eliminating.
US20110294833 Methods for Healthy Aging Genome-wide association studies have been used to elucidate genes and/or pathways related to diseases; however, this methodology has yet to be used to understand the phenotype of healthy aging and/or healthspan in humans.
CA2419801C Steroid derived antibiotics A series of novel steroid derivatives are described. The steroid derivatives are antibacterial agents. The steroid derivatives also act to sensitize bacteria to other antibiotics including erythromycin and novobiocin.
CN101199542A Didanosine dispersing sheet and preparing method thereof The invention discloses a didanosine dispersible tablet and preparation method of the didanosine dispersible tablet. Calculated by weight parts, the didanosine dispersible tablet is made of 100 parts of didanosine, 400 to 500 parts of calcium carbonate, 200 to 300 parts of magnesium hydroxide, 200 to 300 parts of sorbitol, 50 to 100 parts of lactose, 200 to 300 parts of povidone K30, 100 to 150 parts of microcrystalline cellulose, 50 to 100 parts of sodium carboxymethyl starch, 40 to 50 parts of stevia, 10 to 20 parts of magnesium stearate and proper amount of 75 percent of ethanol solution. When in preparation, the didanosine dispersible tablet has high yield and low cost.
CN101991603A Preparation for treating cold in children and preparation method The invention relates to a preparation for treating cold in children, which is prepared from the following components in parts by weight: 4 to 8 parts of cultured in vitro bezoar, 110 to 130 parts of acetaminophen, 0.4 to 0.8 part of chlorpheniramine maleate, 5500 to 6000 parts of cane sugar and 200 to 400 parts of edible essence. Medicaments are mixed and ground by using an equivalent increment method; after the assistant material of the cane sugar is baked at 80 DEG C for 1 hour and then pulverized, mixed powder of the medicaments is mixed and ground by the increment method and granulated; the cultured in vitro bezoar is used for replacing artificial bezoar so that side effects of nausea and jaundice symptoms caused by over-high free bilirubin contained in the artificial bezoar can be reduced; and the equal increment method is used for mixing and grinding so that the medicament components are effectively dispersed and the side effects caused by uneven content of the chlorpheniramine maleate are reduced.
WO2010033941A1 Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors Compounds of Formula (I): in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.
CN102872137A Application of Houttuynoid B in drug for treating cervical cancer The invention discloses application of Houttuynoid B in preparing a drug for treating human cervical cancer, belonging to the technical field of the new use of the drug. Houttuynoid B is found to have obvious inhibition effect on the growth of human cervical cancer cell lines HeLa, HeLa229, HCE1 and CaSKi through MTT (Methyl Thiazolyl Ternzolinm) anticancer activity evaluation in vitro. Therefore, Houttuynoid B can be used for preparing the anti-cervical cancer drug and has excellent prospects in development and application. The use of Houttuynoid B in preparing the drug for treating the human cervical cancer involved in the invention is disclosed for the first time; the framework type of Houttuynoid B is a brand new framework type; and Houttuynoid B has an unexpectedly high inhibition activity for the human cervical cancer cells.
US7049303 Inhibition of viruses Disclosed is a pharmaceutical composition comprising a ribonucleoside analogue in accordance with general formula I or II as herein defined, in admixture with a physiologically acceptable excipient diluent or carrier.
CN103271919A Application of Myriberine A in preparing drug for treating rectal cancer The invention discloses an application of Myriberine A in preparing a drug for treating rectal cancer, and belongs to the technical field of novel drug applications. In-vitro MTT antineoplastic activity evaluation shows that Myriberine A has a significant inhibitory effect for the growth of human rectal cancer cell line LOVE1, LOVO, SW480 and SW620. Therefore, Myriberine A can be used for preparing the drug for treating the rectal cancer and has good development and application prospects. The application of Myriberine A in preparing the drug for treating the rectal cancer is disclosed for the first time. Besides, the Myriberine A has an extraordinary inhibitory activity for rectal cancer cells.
DE102011003315A1 New 1H-pyrazolo(3,4-b)pyridine compounds are guanylate cyclase stimulators useful for treating and/or preventing e.g. heart failure, angina pectoris, hypertonia, pulmonary hypertonia, ischemia, vascular disease, and fibrotic disorder 1H-Pyrazolo[3,4-b]pyridine compounds (I) or their N-oxides, salts, solvate, salts of N-oxide and solvates of N-oxides and salts, are new. 1H-Pyrazolo[3,4-b]pyridine compounds of formula (I) or their N-oxides, salts, solvate, salts of N-oxide and solvates of N-oxides and salts, are new. A : N or CR 3>; R 3> : H, D, F, CHF 2, CF 3, (1-4C)-alkyl, cyclopropyl or cyclobutyl; L : a-CR4AR4B-(CR5AR5B) p-b; a : connection point at carbonyl group; b : connection point to pyrimidine or triazine ring; p : 0-2; either R4A, R5A : H, F, (1-4C)-alkyl or OH; and R4B : H, F, (1-4C)-alkyl, CF 3, (1-4C)-alkoxy-carbonylamino or phenyl, where (1-4C)-alkyl is optionally substituted by 1 or 2 F, CF 3, OH, hydroxycarbonyl or (1-4C)-alkoxycarbonyl; and R5B : H, F, (1-4C)-alkyl or CF 3; or R4AR4BC : 3-6 membered carbocyclic ring, 4-6 membered heterocyclic ring (both optionally substituted by 1 or 2 F or (1-4C)-alkyl), an oxo group or (2-4C)-alkenyl; R 1> : H or F; and R 2> : benzyl substituted by 1-3 F. Independent claims are included for: (1) the preparation of (I); (2) a 3-(1H-pyrazolo[3,4-b]pyridin-3-yl)-[1,2,4]triazin-5-ylamine compound of formula (XV); (3) a 3-(1H-pyrazolo[3,4-b]pyridin-3-yl)-[1,2,4]triazin-5-ol compound of formula (XIII); and (4) a medicament comprising (I), inert and non-toxic auxiliary agent and a further active agent, which is an organic nitrate, nitiric oxide donors, cGMP-phosphodiesterase inhibitors, anti-thrombotic active agents, blood pressure lowering agents and/or fat metabolism modifying agent. [Image] - ACTIVITY : Cardiant; Antianginal; Muscular-Gen.; Vasotropic; Thrombolytic; Antiarteriosclerotic; Antiarrhythmic; Antiparkinsonian; Antiinflammatory; Endocrine-Gen.; Antilipemic; Anorectic; Uropathic; Nephrotropic; Neuroprotective; Hypotensive; Respiratory-Gen.; CNS-Gen.; Nootropic; Cerebroprotective; Anticonvulsant; Antidepressant; Antibacterial; Immunosuppressive; Gastrointestinal-Gen.; Antiarthritic; Antirheumatic; Vulnerary; Hepatotropic; Virucide; Osteopathic; Ophthalmological. - MECHANISM OF ACTION : Guanylate cyclase stimulator. The ability of (I) to stimulate guanylate cyclase was tested using recombinant guanylate cyclase reporter cell line. The results showed that 2-[1-(2-fluorobenzyl)-1H- pyrazolo[3,4-b]pyridin-3-yl]-5,5-dimethyl-5,7-dihydro-6H-pyrrolo[2,3d ]pyrimidin-6-one exhibited a minimal effective concentration of 0.01 mu M.
WO2014101113A1 Piperazine-substituted 7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties Disclosed are compounds of Formula (A), as defined herein, which have binding activity for an A2A-receptor and are believed to be useful for treatment or management of CNS diseases or conditions which can be treated or managed using compounds which have A2A receptor antagonist activity.
CN102657636A Medical application of 4-hydroxylated chalcone in preventing and treating acute lung injury, septicopyemia and inflammation The invention belongs to the technical field of medicines, relates to a medical application of 4-hydroxylated chalcone, and in particular relates to an application of the 4-hydroxylated chalcone in preventing and treating acute lung injury, septicopyemia, inflammation and related diseases.
US20080287443 Treatment of Subgingival Pocket Infections Use of a morpholino compound having the general formula (I) wherein R1 is a straight or branched alkyl group containing (8) to (16) carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing (2) to (10) carbon atoms, substituted with a hydroxy group except in the alpha-position, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment of an infected sub-gingival pocket.
US20050004171 Increasing blood absorption of proton pump inhibitor; adjusting stomach gastric fluid pH with buffering agent to inhibit acid degradation Disclosed herein are methods, kits, combinations, and compositions for treating gastric acid disorders employing pharmaceutical compositions comprising a proton pump inhibiting agent (PPI) and a buffering agent in a pharmaceutically acceptable carrier.
CA2371012C 4-(1h-pyrrol-1-yl) imidazoles The invention comprises a novel 4-(1H-Pyrrol-1-yl) imidazole having the following general structural formula:(see formula I) These compounds are useful intermediates in the preparation of pharmaceutical compounds for use in treating hypertension and related medical conditions.
CN101919839A Usage of mangiferin calcium salt taken as AMPK agonist The invention provides a usage of mangiferin calcium salt for preparing AMPK agonist. The mangiferin calcium salt has the structure shown by the following formula.
EP1071668B1 5-aminoindeno[1,2-c]pyrazol-4-ones as anti-cancer and anti-proliferative agents The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I), that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits known as cyclines A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
CA2255539C Therapeutic uses of bpi protein products in humans with hemorrhage due to trauma Methods and materials for the treatment of humans suffering from hemorrhage due to trauma are provided, in which therapeutically effective amounts of BPI protein products are administered.
WO2006121391A1 New compounds i A compound of formula (I), or pharmaceutically acceptable salts thereof wherein X is selected from hydrogen, halo, -CN, -CON2, -CON(C1-6alkyl)H, -CON(C1-6alkyl)2 and heterocyclic groups; R1 is selected from C1-6alkyl and C3-6cycloalkyl; whereby Z is -OH, M is selected from C(O)- , -CH(ORa) , N(Ra) , and S(O)r-, wherein Ra is hydrogen or C1-6alkyl and r is 0, 1 or 2, R2 is selected from C1-6alkyl, C3-6cycloalkyl, heterocycloalkyl, aryl, alkylaryl, and heteroaryl, R2 is substituted with halo, -NO2, -CN, -OH, -CF3, -OCF3, -NH2, and/or -CONH2, when Y is -C1-6alkyl; or Z is -C1-6alkoxy, M is bond, R2 is selected from C1-6alkyl, C3-6cycloalkyl, heterocycloalkyl, aryl, alkylaryl, and heteroaryl, when Y is -C1-6alkoxy.
CN102670706A Paste for treating soft tissue injury, osteoproliferation and pain in waist and lower extremities The invention relates to a paste for treating soft tissue injury, osteoproliferation and pain in waist and lower extremities, which is prepared from the following raw materials in parts by weight: 10 parts of borneol, 5 parts of camphor, 20 parts of dried alum, 30 parts of realgar and 5 parts of menthol crystal. The preparation method of the paste comprises the following steps: preparing the raw materials and grinding the raw materials to fine powder for later use; cutting 100 parts of raw rubber into strips with proper size, smelting the strips into netty rubber sheet in a rubber mixing mill, naturally cooling, soaking the netty rubber sheet in 300 parts of gasoline for 18-24h until the rubber sheet completely swells into gel, transferring the gel into a pasting barrel, stirring for 3-4h, sequentially adding 10 parts of vaseline, 100 parts of rosin and 5 parts of vegetable oil, and then adding 150 parts of zinc oxide to prepare a substrate, and finally adding 100 parts of medicine powder, continuously stirring for 4h to form uniform paste pulp, spreading, recycling the solvent, and packaging to finally obtain the paste. The paste disclosed by the invention has the advantages of low preparation cost, good effect and little by-effect.
CN102731394A Substituted quinoline-2-formaldehyde-phenylhydrazone derivative, and preparation method and application thereof The present invention relates to a substituted-quinoline-2-formaldehyde-phenylhydrazone derivative and a preparation method and application thereof, and in particular relates to a novel 4-acyl-quinoline-2-formaldehyde-phenylhydrazone derivative, and a preparation method and application thereof to preparation of therapeutic drugs for dengue fever and dengue hemorrhagic fever caused by dengue virus. A structure of the compound is shown as a formula 1. The compound can be used as a protease inhibitor for a dengue virus NS2B-NS3, so as to block further proliferation of the dengue virus in a host.
CN102228431A Self-emulsified medicinal composition for taxane compounds The invention provides a self-emulsified medicinal composition for delivering a taxane medicine and a preparation method thereof. The self-emulsified medicinal composition is transparent liquid, contains an effective amount of taxane compounds, oil components, surfactant and ethanol, and preferably contains lactic acid, wherein the surfactant is phospholipid and cremophor EL. Microemulsion with the average particle size of between 50 and 300nm can be formed through self-emulsification by adding the self-emulsified composition into a glucose injection; and the microemulsion can stabilize for more than 12 hours at room temperature. In the method, the preferable taxane compound is taxol.
CN101474411B Anti-tumor prodrug using novel amphipathic hyperbranched polyesters as carrier and preparation method The invention provides an antitumor prodrug with novel amphiphilic hyper branched polyester as a carrier and a preparation method thereof. The novel biodegradable amphiphilic hyper branched polyester is constructed as being based on dimethylol propionic acid, an oligomer of glycolic acid or lactic acid and polyethyleneglycol or polyethylene glycol monomethyl ether. A peripheral functional group of the obtained hyper branched polymer is a hydroxyl group. The hyper branched polymer is reacted with estolide to be transformed into the hydroxyl group, the hydroxyl group is esterified with antitumor drug with the existence of condensing agent to obtain a prodrug of the antitumor drug. The introduction of the oligomer of the glycolic acid or the lactic acid or an alternative oligomer thereof improves the biocompatibility of drug carrier material, and the degrading speed of the oligomer in body is controlled by regulating the polymerization degree and the chemical composition of the oligomer to realize the action of controlling the release speed of the drug, so that the invention has very good drug sustained controlled release action and avoids the toxic side effect to normal cells causedby the burst release of the antitumor drug. The prodrug has an amphiphilic property, so that the prodrug can be made into a water-based preparation and improves the hydrophilicity of the antitumor drug greatly.
CN101822824A Marine organism sterilizing and cleaning liquid for animal bites, scratches and licking wounds The invention relates to a marine organism sterilizing and cleaning liquid for animal bites, scratches and licking wounds, which is especially used for cleaning and sterilizing human wounds caused by the biting, the scratching and the licking of animals and pets. The invention is a safe and reliable marine organism type product which integrates sterilization and cleaning and has good effect and no poison or harm.
CN101328154B 3-alcoxymethyl amidine-1,2,4-benzotriazin derivates, preparation and use thereof The invention provides a 3-alkoxyl oxygen methyl amidine-1, 2, 4-phentriazine derivative. 3-amino-phentriazine-1-single oxide (II) and aldehyde are put into an excessive alcoholic solution and are heated to react, and a single oxide is oxidized by m-chloroperoxybenzoic acid to get the final product of 3- alkoxyl oxygen methyl amidine-1, 2, 4-phentriazine-1, 4-dioxide (IV). The synthesized compound has raw materials available easily, simple process and high total yield; the provided derivative not only improves the hypoxia antitumor activity and but also improves the hypoxia antitumor selectivity. In addition, the ability of the vein to diffuse externally is improved evidently and the derivative can be applied to the preparation of antitumor medicines. The structural formula of the derivative is shown above.
US7026324 Amide containing a pyridinone or pyrazinone compound as serine protease enzyme inhibitors Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein R2 is R3 is selected from the group consisting of 1) hydrogen, 2) halogen, 3) C1–4 alkyl, 4) C3–7 cycloalkyl, 5) CF3, 6) OCF3, 7) C1–4 alkoxy, and 8) cyano; and R12 is a 5-membered heteroaryl ring having 2, 3, or 4 heteroatoms, provided that at least 1 heteroatom is N, and at most 1 of the heteroatoms is S, said ring being unsubstituted or substituted, at any one ring atom, with CH3 .
CN102008663A Oral liquid for preventing heatstroke and reducing temperature for livestock and poultry and preparation method thereof The invention relates to oral liquid for preventing heatstroke and reducing temperature for livestock and poultry and a preparation method thereof. The oral liquid is characterized by consisting of the following medicaments in part by weight: 5 to 9 parts of gypsum, 8 to 12 parts of rhizoma anemarrhenae, 8 to 12 parts of wrinkled giant hyssop, 5 to 9 parts of liquorice, 30 to 35 parts of rhizoma phragmitis and 30 to 35 parts of watermelon peel. The preparation method comprises the following steps of: weighing the medicaments serving as raw materials in part by weight, namely weighing the six medicaments serving as the raw materials in part by weight; adding water in an amount which is 4 times weight of the medicaments, decocting twice, combining the decoction per 1.5 hours, filtering, standing the filtrate for 12 hours, and taking the supernatant for concentrating; and adding ethanol until the alcohol content is 60 percent, standing, filtering, adding water, filtering, sealing and making the steam flow at the temperature of 100 DEG C for 30 minutes. The invention has the advantages that: each component in the formula plays a role in preventing heatstroke and reducing temperature together, changes the current situation that medicaments for preventing heatstroke and reducing temperature in livestock and poultry industry are monotonous and insufficient, and the composition has the characteristics of high security coefficient, quick response, exact curative effect, no medicinal residue and no toxic or side effect.
CN102895202A Cefetamet pivoxil hydrochloride dispersible tablet and preparation method thereof The invention relates to the field of a medicine, in particular to a cefetamet pivoxil hydrochloride dispersible tablet and a preparation method of the cefetamet pivoxil hydrochloride dispersible tablet. The cefetamet pivoxil hydrochloride dispersible tablet is prepared by the following components in parts by weight: 40 to 60% of cefetamet pivoxil hydrochloride, 10 to 20% of microcrystalline cellulose, 5 to 15% of polyvinylpolypyrrolidone, 5 to 12% of calcium hydrophosphate and 5 to 15% of carboxymethyl starch sodium. Compared with the ordinary tablet, the cefetamet pivoxil hydrochloride dispersible tablet provided by the invention has the advantages of being good in disperse state, short in disintegration time, high in bioavailability, little in untoward effect, rapid to dissolve the medicines, fast to absorb and convenient to take and the like.
CN102988716A Medicament for treating aestates The invention relates to a medicament for treating aestates. The medicament is characterized by being prepared from the following raw materials in parts by weight: 20-40 parts of red phaseolus beans, 250-350 parts of mung beans, 6-8 parts of radix angelicae, 3-5 parts of steatite, 10-20 parts of lilium brownie, 6-8 parts of rhizoma typhonii and 3-5 parts of radix saposhnikoviae. The medicament is prepared as follows: crushing the red phaseolus beans, the mung beans, the radix angelicae, the steatite, the lilium brownie, the rhizoma typhonii and the radix saposhnikoviae, grinding the mixture to be powders, mixing uniformly, and bottling for standby. When the medicament is used, 15g of medicine powder is taken for each time, is added water and mixed uniformly, and the mixture is smeared for 2 times each day. The medicament has compatibility of medicines, clears heat and dispels wind, moistens skin and removes freckles and is suitable for treating freckles, pachulosis, acne rosacea and the like, and particularly has a good aestates treat effect.
EP2101798A2 Topical treatment of acne with extracts of glycyrrhiza, foeniculum and atriplex, combined with minerals A composition for topical treatment of various forms of acne comprising 20-40% by volume of alcohol extracted GLYCYRRHIZA GLABA plant, 15-30% by volume of alcohol extracted FOENICULUM OFFICINALE plant, 15-45% by volume of saturated water solution of mineral salts selected from the group of NaCl and/or KCl and/or MgCl2, and 1-3% by volume of alcohol and water extracted ATRIPLEX HALIMUS plant. The plant extracts may be admixed with SULFUR and the composition may be further comprised of 6-10% by volume of a solvent such as alcohol and 8-12% by volume of water.
US8097607 loading-dose regimen; an initial administration of rifalazil for 4 to 14 days, followed by less than half this average daily dose for the subsequent 4 to 14 days The invention features low-dosage rifalazil compositions which are useful for the treatment of bacterial infections.
CN1616428A Acenaphthene heterocyclic compound and its cell fading inducing and anti-tumor use The present invention relates to a kind of amino group or halogen substituted 8-oxy-8H-acenaphthenee[1, 2-b] pyrrolyl-9-nitrile derivatives and their biological use. They are applied mainly in intracorporeal and extracorporeal inducing cell apoptosis and as anticancer compound. These compounds are 3, 6-disubstituted, 3-disubstituted or 6-substituted 8-oxy-8H-acenaphthenee[1, 2-b] pyrrolyl-9-nitrile derivatives. They can induce tumor cell apoptosis and block cell period in the dosage dependent mode within the wide concentration range of 0.01-10 micro mole. The highest activity compound B1 has IC50=0.17 micro mole (0.56 micro gram). When they are used in animal tumor model body, they can inhibit tumor growth obviously in inducing cell apoptosis mode. Therefore, the present invention is one kind of apoptosis inducing agent and antitumor compound with high activity.
US20110245235 Systems, Methods, and Devices for Rehabilitation of Auditory System Disorders Using Pharmaceutical Agents and Auditory Devices The present inventions provide combination therapies, kits, and methods for providing relief and/or for improving one or more symptoms associated with an auditory system disorder in a subject diagnosed with the auditory system disorder, comprising an effective amount of at least one pharmaceutical agent and at least one auditory system disorder device, as well as methods for using at least one pharmaceutical agent and/or at least one auditory system disorder device in the manufacture of said kits.
CN1943580A New use of fumigacin type steroids in producing medicine for anti-drug fast bacteria The invention discloses a new uses of helvolicacid sterides in making drugs of antibiotic-resistant microbes, including helvolicacid, fusidic acid and its salt and salt hydrates acceptable in pharmacology, compound of ester or prodrug with single or multi-antibiotic, applying to preparation of drugs of antibiotic-resistant microbes.
CA2622541C Use of fluorinated triazoles for treating neuropathic pain The present invention relates to the use of fluorinated triazoles of the formula I: (see formula I) for treating neuropathic pain.
US20090209596 Oxazole Hydroxamic Acid Derivatives and Use Thereof Provided are an oxazole hydroxamic acid derivative and a pharmaceutically useful salt thereof as a histone deacetylase inhibitor The oxazole hydroxamic acid derivative and pharmaceutically useful salt thereof, prepared in accordance with the present invention, can treat and/or prevent various cancers and inflammatory diseases caused by histone deacetylase.
US20120095020 Cathepsin S Inhibitor Compounds The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also, the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier. The present invention further provides methods for treating abdominal aortic aneurysm, plaque instability, atherosclerosis, or autoimmune disorders such as rheumatoid arthritis, psoriasis, and lupus comprising administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable diluent or carrier.
CA2543115A1 Compositions and methods for detecting and treating diseases and conditions related to chemokine receptors Ligands of CCX-CKR2 and the biological role of CCX-CKR2 in cancer is described.
WO2013078754A1 Promoting hair growth solution containing chlorine dioxide， preparation method and use method thereof An externally used solution containing chlorine dioxide for promoting hair growth is composed of chlorine dioxide or its precursor, pH regulator, medical solvent and plant extract according to certain weight ratio. The product may take the forms of a single solution containing chlorine dioxide or several solutions comprising chlorine dioxide precursor. The safety and efficient oxidation sterilization and tissue regeneration ability of chlorine dioxide are introduced into the solution system for promoting hair growth, and the steps of removing hair loss factors, stimulating the growth of hair follicles, anti-inflammatory and anti-dandruff are done synchronously. Complemented Medical solvent and plant extracts, change alopecia environment.
CN103193691A Sulfonamide compound and medicinal compositions thereof, and preparation methods and applications thereof The invention discloses a sulfonamide compound and medicinal compositions thereof, and preparation methods and applications thereof. The sulfonamide compound can be used as a micro-molecular tubulin inhibitor, has an anti-microtubule effect in vitro, can induce the apoptosis of tumor cells in vitro, has an obvious inhibition effect on multidrug resistance cells in vitro, and has a substantial in-vivo oral antitumor activity. Additionally, the compound has the advantages of small molecular weight, simple synthesis, and small toxic side effects. The invention also provides medicinal compositions containing the sulfonamide compound and pharmaceutically acceptable salts thereof as an active component.
CN101143126A Ethyl cellulose slow release system for nucleophilic NO donor medicine and its preparation method The invention belongs to the medicinal engineering technical field and concretely relates to a slow-release system and the preparation method of a nucleophilic (NO) donator drug. The invention uniformly disperses the hydrophilic and nucleophilic (NO) donator drug into ethyl cellulose solution to obtain a single-layer drug film or a three-layer drug film. The slow-release film of the nucleophilic (NO) donator drug can obviously increase the stability in buffer solution of the hydrophilic and nucleophilic (NO) donator drug and obviously prolongs the release period and conquers the disadvantages of the novel (NO) donator drug that the hydrolysis is prompt; the half life is short; the (NO) donator drug can be difficultly stable in aqueous solution; the release is slow. The slow-release system can satisfy the requirements of the (NO) release velocity and the release period for remedying cardiovascular disease and can be used to prepare a drug bracket and a film material which is provided with the target-oriented control and release of the nucleophilic (no) donator, so the slow-release system has important clinical application value and application prospect.
US8575186 Epiminocycloalkyl[b] indole derivatives as serotonin sub-type 6 (5-HT6) modulators and uses thereof The present invention relates to epiminocycloalkyl[b]indole derivatives as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, and methods of preparation and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, and schizophrenia. The subject compounds have the structure of formula (I) with the substituents being described herein.
US20080119488 Modulators Of Nuclear Receptors Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
US8227200 Methods for identifying kremen polypeptide binding partners The present invention relates to a composition useful for the diagnosis and therapy of diseases associated with aberrant expression of the gene encoding the receptor Kremen 1 and/or Kremen 2 e.g. tumors or diseases of the kidneys, bones and eyes, lipid and glucose metabolism and obesity. The present invention also relates to a pharmaceutical composition containing a compound which is capable of modifying (a) the expression of the gene encoding Kremen 1 and/or Kremen 2 or (b) the activity of the Kremen 1 and/or Kremen 2 receptor.
CN101347443A Vitamin B12 in situ forming eye gel The invention discloses a vitamin B12 forming gel for eye use and a preparation method thereof. 1,000ml vitamin B12 forming gel for eye use of the invention contains 100 to 250mg of vitamin B12, 0.05 to 1g of antiseptic, 1.0 to 7.5g of osmoregulator, 30 to 150g of gel matrix and the rest of acid-base buffering agent and injection water. The invention, with the optimization of auxiliary materials and the improvement of process, enriches the dosage forms of vitamin B12, greatly extends the staying time in eyes of the medicine and improves the curing effect without adverse stimulus responses.
WO2010004517A1 Triazole derivatives useful for the treatment of diseases The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
WO2005027937A1 Glycolipid-containing composition, use thereof and process for producing the same A glycolipid-containing composition which can be purified by a convenient method from, for example, spinach (Spinacia oleracea L.) and contains three glycolipids, i.e., monogalactosyl diacyl glyerol, digalactosyl diacyl glycerol and sulphoquinovosyl diacyl glycerol at a high ratio. This glycolipid-containing composition has useful physiological activities such as a DNA synthase inhibitory activity, a cancer cell growth inhibitory activity and an antitumor activity. When treated with a lipase, its shows further enhanced physiological activities and, therefore, becomes useful in, for example, functional foods having an anticancer effect or a cancer preventing effect.
CN103491972A Granules in liquid dosage form A preparation comprising coated granules and a water-soluble gel, said preparation being characterized in that: the coated granules comprise an oil-absorbing agent; the oil-absorbing agent comprises cashew nut shell liquid, anacardic acid, cardanol or cardol; and the coated granules are suspended in the water-soluble gel.
US7112581 For therapy of cancer and infectious disease Compounds represented by the following structure (I), acid-addition salts and pro-drugs are disclosed: wherein the ring structure includes no substitutions, one substitution, or more than one substitution; and wherein n is equal to an integer grater than 1, preferably 2, 3, or 4; m is equal to a positive integer, preferably 1, 2 or 3, and each separate Xn and X are each separately selected from a nucleophilic residue, preferably —H, —OH, —O—CO-alkyl, —O-alkyl, —NH2, a halogen and the like; and wherein the dashed line represents a C—C bond or a C—H bond, and the dashed and solid line represents either a carbon-carbon single bond or a carbon-carbon double bond.
US20110281796 Novel activin receptor and uses thereof The present invention provides novel activin IIB5 receptor polypeptides capable of binding and inhibiting the activities of activin A, myostatin, or GDF-11. The present invention also provides polynucleotides, vectors and host cells capable of producing the receptor polypeptides. Compositions and methods for treating muscle-wasting, metabolic and other disorders are also provided.
US20100120744 Acetamidopropane modulators of nmda receptors The present invention relates to new acetamidopropane modulators of NMDA receptor, pharmaceutical compositions thereof, and methods of use thereof.
US20090317391 Cancer Related Genes (PTPE) This invention is in the field of cancer-related genes. Specifically it relates to methods for detecting cancer or the likelihood of developing cancer based on the presence or absence of the tm-PTPε gene or proteins encoded by this gene. The invention also provides methods and molecules for upregulating or downregulating the tm-PTPε gene.
WO2011083304A1 Prodrugs of opioids and uses thereof The present invention concerns prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing more consistent pain relief by increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are provided. The invention also provides for decreasing the adverse GI side effects of opioid analgesics.
US20100008966 Medical Devices and Methods for Delivery of Nucleic Acids Embodiments of the invention include devices for the release of nucleic acids and related methods. In an embodiment, the invention includes an active agent eluting coating including a polymeric matrix, a cationic carrier agent disposed with the matrix, and an active agent disposed within the matrix, the active agent including nucleic acids substantially uncomplexed with the cationic carrier agent. In an embodiment, the invention includes a method of making an implantable medical device including selecting a concentration of a cationic carrier agent corresponding to a desired elution profile, combining a matrix forming polymer, an active agent, a solvent, and the cationic carrier agent to form a coating composition having the selected concentration of the cationic carrier agent, the active agent comprising nucleic acids, and depositing the coating composition onto the surface of a substrate. Other embodiments are included herein.
EP1047416B1 Pharmaceutical compositions comprising disulfiram for inhibiting angiogenesis Disulfiram (tetraethylthiuram disulfide) is shown to inhibit angiogenesis and to be useful in the treatment of angiogenesis-dependent disorders, including neoplasms, and to prevent cell hyperproliferation and formation of clots along or around medical devices.
WO2009090399A1 Indoles active on crth2 receptor Indole derivatives having therapeutic utility are of formula (I): X is -SO2- or *-SO2NR3- wherein the bond marked with an asterisk is attached to Ar1; R1 and R2 are, independently, hydrogen, fluoro, chloro, CN or CF3; R3 is hydrogen, C1-C8alkyl or C3-C7cycloalkyl; and Ar1 and Ar2 are, independently, phenyl or a 5- or 6-membered heteroaryl group, wherein the phenyl or heteroaryl group is optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C7cycloalkyl, -O(C1-C4alkyl) or C1-C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.
WO2014144097A1 Antifungal drugs The present invention relates to the administration of compounds of formula (I) for the treatment and/or prevention of fungal infections in subjects in need thereof. The methods of the invention also relates to the administration of pharmaceutical compositions comprising compounds of formula (I) for the treatment and/or prevention of fungal infections in subjects in need thereof. Subjects suffering from fungal infection and immunocompromised subjects may particularly benefit from the methods and compositions of the invention.
US20120058966 Sphingosine Kinase Inhibitor Prodrugs The invention relates to prodrugs of hydroxyl-substituted adamantane compounds, pharmaceutical compositions thereof, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
CN102552208A Daidzein solid dispersion micro-pill capsule and preparation method thereof The invention relates to a daidzein solid dispersion micro-pill capsule and a preparation method thereof. The daidzein solid dispersion micro-pill capsule comprises daidzein and a pharmaceutic adjuvant and is characterized in that water is used as a preparing solvent, the pharmaceutic adjuvant comprises blank pill cores, a cosolvent and a solid dispersion carrier material, and each capsule is composed of 50mg of daidzein, 25-100mg of cosolvent, 50-150mg of povidone K30 and 50-100mg of blank pill cores. According to the preparation method, organic solvents such as ethanol are not used so that the anti-explosion problem in production is solved; and simultaneously, through the combination of the cosolvent and a solid dispersion technology, the problems such as low dissolution rate of gastricacid in the cosolvent addition technology, overmuch usage amount of a carrier material in a solid dispersion technology are solved, and the stability and bioavailability of the product are obviously increased.
CN103705457A Valnemulin hydrochloride/polyethylene glycol drug-loaded particle-containing glycol oily injection The invention relates to a valnemulin hydrochloride/polyethylene glycol drug-loaded particle-containing glycol oily injection which is prepared by composing valnemulin hydrochloride and solid polyethylene glycol to drug-loaded particles and suspending the drug-loaded particles in an oily medium. Polyethylene glycol with molecular weight larger than 6000 is preferably selected for preparing the preparation, and any one of tetradecanoic acid isopropyl ester, injection soybean oil, corn oil and tea-seed oil is preferably selected for preparing the preparation. Hydroxypropyl methyl cellulose or high-substituted hydroxypropyl cellulose is also added in the preparation.
US20100063017 Ophthalmic Suspension for Ocular Use A gatifloxacin and prednisolone topical ophthalmic pharmaceutical compositions for prevention and treatment of ophthalmic bacterial infections and inflammatory conditions associated with pre-surgical and/or post surgical ocular surgeries.
US20100286165 Substituted oxindole compounds The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
CN103040785A Permeable gastric retention tablets and preparation method thereof The invention belongs to the technical field of medicines, and in particular relates to a preparation method of permeable gastric retention tablets. The gastric retention tablets can be single-layer tablets or double-layer tablets. The single-layer permeable gastric retention tablets are prepared by the following steps of: pressing medicaments and a penetration enhancer or macromolecular accessories into solid tablet cores with the diameters of 10 to 22 millimeters; wrapping a layer of cellulose acetate semi-permeable membrane outside each solid tablet core to form a coating; and opening one or more medicament release pores in the coatings by laser or by hand. The double-layer permeable gastric retention tablets are formed by adding a push layer on each single-layer permeable gastric retention tablet and opening a medicament release pore in one side of a medicament contained layer. After the permeable gastric retention tablets are orally taken, the original size of the tablets can be kept all the time in the release process, and the tablets can be retained in the stomach of a patient for a long time; and the release of the permeable pump tablet medicament is at a zero level, so that the blood concentration is relatively stable.
CN1768752A Sustained release formulation with cetirizine and pseudoephedrine hydronate The invention relates to a slow release preparation of Certirizine and Pseudoephedrine Hydrochloride, wherein optimum formulation being, the pesudoephedrine hydrochloride slow release layer comprises d-pesudoephedrine hydrochloride 120g, HPMC60RT1000 20g, HPMC60RT10000 80g, crystalline cellulose 60g, right amount of 10% polyvinyl pyrrolidon anhydrous alcohol liquid, magnesium stearate 2g, the Certirizine hydrochloride quick release prescription includes Certirizine hydrochloride 5g, crystalline cellulose 80g, lactin 80g, sodium carboxymethylstarch 20g, right amount of 10% polyvinyl pyrrolidon anhydrous alcohol liquid, and magnesium stearate 1g.
EP1575585A1 Pharmaceutical liquid composition containing pyridone derivative A pharmaceutical liquid composition containing the Pirfenidone in a very high concentration of more or less 25% by weight can be obtained by dissolving the Pirfenidone in diethylene glycol monoethyl ether. Even when the liquid medicinal compositions are stored for a long period of time, the Pirfenidone will not be recrystallized with a good chemical and physical stability. Furthermore, the liquid compositions are little irritating to the wounds on the mucous membrane of the skin and suitable for the manufacture of pharmaceutical formulations to be administered either via the oral, percutaneous, nasal or vaginal routes or by means of spray, patch, inhalation, injection or intravenous drip.
CA2353808C Agent for lowering endothelin levels The present invention relates to a new medical use of triphenylethylene antiestrogen toremifene or a pharmaceutically acceptable thereof for lowering endothelin-1 levels in mammals, and for the prevention or treatment of endothelin mediated diseases.
US20120107775 Methods of Using Botanical-Based Compositions to Treat Microbial Dental Disease The present invention relates to methods of using botanical-based compositions to treat or prevent microbial dental disease. The claimed invention is directed to methods of using botanical-based compositions in a rinse, gel- or paste-like form to prevent microbe invasion of dental cavities, including the root canal.
EP1830832A1 Zinc-containing treatments for hyperphosphatemia A method of treating hyperphosphatemia in a subject comprises the step of administering to the subject an effective amount of a pharmaceutically acceptable zinc salt. A pharmaceutical composition comprises a pharmaceutically acceptable carrier, a pharmaceutically acceptable zinc salt; and a phosphate sequestrant. In one embodiment, the phosphate sequestrant is selected from a pharmaceutically acceptable lanthanum, calcium, magnesium and iron salt. In another embodiment, the phosphate sequestrant is an amine polymer, wherein the molar ratio of a zinc ion of the ion salt to amine nitrogen atoms in the amine polymer is 0.1-3.0. The invention also includes a pharmaceutical composition comprising a pharmaceutically acceptable carrier; a pharmaceutically acceptable zinc salt; and an agent selected from the group consisting of a phosphate transport inhibitor, and HMG-CoA reductase inhibitor and an alkaline phosphatase inhibitor.
EP2776397A1 Quinolines as fgfr kinase modulators The invention relates to new quinoline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. Formula (I)
US20080118462 Biomarkers for Melanoma The present invention relates to methods of determining melanoma status in a subject. The invention also relates to kits for determining melanoma status in a subject. The invention further relates to methods of identifying biomarker for determining melanoma status in a subject.
US20080119403 Haparin-Binding Protein Modified with Heparan Sulfate Sugar Chains, Process for Producing the Same and Pharmaceutical Compositions Containing the Same A heparin-binding protein having covalently bonded heparan sulfate sugar chains within its molecule is produced by ligating a cDNA encoding a peptide which can be modified with heparan sulfate sugar chains selectively to a cDNA encoding a heparin-binding protein and producing in an animal cell the gene product of the resultant ligated cDNA. This heparan sulfate sugar chain-modified heparin-binding protein is functionalized by covalently bonding thereto glycosaminoglycan sugar chains containing little chondroitin sulfate. For example, this heparin-binding protein is excellent in stabilities, such as thermostability, acid resistance, alkali resistance and in vivo stability. Further, the heparan sulfate sugar chain-modified heparin-binding protein is effective in cell proliferation and tissue regeneration, and has effect of regulating the physiological functions of FGFs. Thus, this heparin-binding protein is extremely useful as a medicine for preventing or treating various FGF-related diseases.
EP0979817B1 Leukotriene a4 hydrolaze inhibitors Leukotriene A4 hydrolaze inhibitors containing a compound of general formula (I) or a salt thereof as the active ingredient, wherein R1 represents hydrogen, alkyl, phenylalkyl, alkanoyl or benzoyl; R?2 and R3¿ each represent hydrogen or alkyl; R4 represents hydroxyl, alkoxyl, phenylalkoxyl, amino, alkylamino or phenylalkylamino; R5 represents phenylalkyl or naphthylalkyl; Z represents sulfur or oxygen; A represents alkylene; and n represents 0, 1 or 2, provided that the phenyl ring in R1 may be substituted with alkyl, alkoxyl or halogen, and that the phenyl ring or naphthyl ring in R5 may be substituted with alkyl, cycloalkyl, alkoxyl, alkylthio or halogen.
CN1569021A Enteric-coated azithromycin preparation and its preparing process The invention discloses an enteric-coated azithromycin preparation and its preparing process, which comprises effective dosage of azithromycin or medicinal excipient, wheein the medicinal excipient include surface active agent, bulking agent, crumbling agent, lubricating agent, moistening agent or binding agent, intestine solution dressing material and plasticizer.
WO2009006799A1 A pharmaceutical compositon comprising taxanes, the preparation and use thereof A pharmaceutical composition comprising therapeutic amount of taxanes, surfactant, latent solvent and stabilizing agent, wherein the latent solvent is selected from one or more of glycerin, polyethylene glycol, or propylene glycol, and the stabilizing agent is sulfoacid or sulfonate, or a mixture of different sulfonates. The composition is injection or frozen powder injection. The compositon can improve the solubility and stability of taxanes. The preparation and use of the pharmaceutical composition are also disclosed.
CN101337071B Composition for preparing anti-cataract products The invention relates to composition which can be used for preparing an anti-cataract product. According to the time phase change of crystalline, the inventor discovers the change law of crystalline Beta B2 with special expression and special distribution along with the organism aging process, determines that crystalline Beta B2 is the target protein more suitable for cataract resistance, and discovers that dithiothreitol is the material which can effectively restrain the heat denaturation of crystalline, such as Beta B2, and then develops the composition composed of glycosylation modification resistant materials, oxidation resistant materials and heat denaturation resistant materials with the target protein as the target spot, in order to prepare the corresponding anti-cataract product. The cataract disease becomes an important pathogenesis which affects the living standard in China, the invention develops the composition which is applicable in preparing the anti-cataract product, and provides a new medicine resource. On the application, the precaution is the key point, the medicine is applied associatively, and is for external administration, thereby the application is wide, theanti-cataract product is an effective product for preventing, diagnosing and treating crystalline denaturation or cataract and the related diseases, and can bring remarkable social benefit and economic benefit.
WO2010116270A1 Ep2/4 agonists EP2/4 compounds having improved dual pharmacological activity are described. The uniqueness of using EP2/4 dual agonists resides in their ability to modify both uveoscleral outflow via the ciliary muscle and conventional outflow via trabecular meshwork and Schlemm's canal all in the same treatment paradigm. The compounds can be employed for the treatment of glaucoma and ocular hypertension. Formula (I).
US20130035365 Anti-sense oligonucleotides targeted against exon 9 of IL-23R alpha gene and method of using same to induce exon skipping and to treat inflammatory bowel diseases The present invention relates to anti-sense oligonucleotides (AONs) used to induce exon 9 skipping in IL-23Rα gene. Exon 9 skipping of the IL23Rα gene ultimately causes specific induction of a novel soluble truncated IL-23Rα (Δ9) protein, characterized by a lack in a transmembrane domain and has a unique eight (8) amino acids (GLKEGSYC) at its C-terminus end as a result of frame-shift. The present invention provides a utility application of the use of AONs to induce production of a Δ9 protein which inhibits IL-23R-mediated cell signaling. More particularly, Δ9 protein blocks STAT3 formation as well as Th17 maturation. There is provided a therapeutic application of AONs in treating a mammal such as a human patient inflicted with Crohn's disease.
EP1049676B1 4- aryl(piperidin-4-yl)] aminobenzamides which bind to the delta-opioid receptor 4-[aryl(piperidin-4-yl)] aminobenzamides are delta-opioid receptor agonists/antagonists of formula (I). As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their agonist/antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of mental illness, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents, and agents for the treatment of respiratory diseases. In formula (I), [Ar is phenyl, 1-naphthyl or 2-naphthyl, each optionally substituted with 1 to 3 R?7; R1 - R8¿ are described in the application].
US20110152340 Methods for Identifying Subjects With an Increased Likelihood of Responding to DPP-IV Inhibitors The invention provides novel in vitro diagnostic methods for identifying subjects or patients who may have an increased likelihood of responding to DPP-IV inhibitor therapy. The invention also provides novel polynucleotides associated with increased responsiveness of a patient to DPP-IV inhibition. Polynucleotide fragments which comprise at least one polymorphic locus, are also provided. Allele-specific primers and probes which hybridize to these polymorphic regions, and/or which comprise at least one polymorphic locus are also provided. The polynucleotides, primers, and probes of the invention are useful in phenotype correlations, medicine, and genetic analysis.
US20080312286 Indanone Potentiators of Metabotropic Glutamate Receptors The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
US7074907 Plant extracts; antioxidant ; stability; whitening agent ; foods, cosmetics The compound of the present invention is a component originated from a natural material, camu camu (Myrciaria dubia), has strong antioxidative activity and stable whitening effect, and is represented by the formula (1). The antioxidant, whitening agent, skin preparation for external use, cosmetics, and food of the present invention are characterized by the inclusion of the compound represented by the formula (1)
WO2011140608A1 Neuropsychopharmacological treatment regimes for treating psychological disorders Neuropsychopharmacological treatment regimes are provided for treating a range of psychological disorders including depression and their sub-threshold forms. A number of treatment protocols are disclosed, comprising a synergistic combination of oxytocin and oestrogen which target the hypothalamopituitary adrenal axis, in combination with antidepressant agents. These treatment protocols may be used alone or in combination with other behavioural modification therapies, for the treatment of psychological disorders such as depression and symptoms of depression. Compositions, medicaments and agents comprising combinations of oxytocin, oestrogen and anti-depressants are also disclosed.
WO2012160006A1 Antagonists of cb1 receptor. The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.
CN101961352A Self-emulsified fish oil soft capsules without fishy smell The invention provides self-emulsified fish oil soft capsules without fishy smell, which comprise scarfskin and inclusion. The soft capsules are characterized by consisting of the following components in part by weight: 85 to 98 parts of fish oil, 0.01 to 0.5 part of vitamin E, 1 to 10 parts of tea chlorophyll and 1 to 5 parts of emulsifying agent. The soft capsules have the advantages of capability of self-emulsifying, high bioavailability, no fishy smell, good mouthfeel and convenience for administration.
WO2013167782A1 Amphiphilic copolymers carrying alpha-tocopherol having antitumoural properties The invention relates to the use of a family of amphiphilic copolymers that form polymeric micelles of a micrometric or nanometric size and consist of acrylic monomers derived from the alpha-tocopherol molecule and highly hydrophilic monomers. This family of copolymers exhibits an antitumoural activity per se, but they can also act as vehicles for other active principles having an antitumoural effect.
US20120195980 Method, Composition and Package for Bowel Cleansing The present invention provides a highly palatable colon cleansing formulation that utilizes a low chloride electrolyte-replenishing base solution. When formulated with polyethylene glycol and a selected sugar alcohol, the formulation offers the advantages of superior palatability without undesirable concomitant side effects or a decrease in cleansing efficacy.
US20090197860 Biaryl substituted diazabicycloalkane derivatives The invention relates biaryl substituted diazabicycloalkanes, and more particularly bicycloheteroaryl substituted fused diazabicycloalkane derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions.
WO2014040052A3 Glycyrrhetinic acid derivatives with anti-inflammatory activity The present application relates to: (a) compounds of Formula (I): and salts thereof, wherein Y and Z are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use for the treatment and prevention of diseases such as those associated with oxidative stress and inflammation.
EP0885060B1 Solid or semi-solid hydrocarbon gels A solid or semi-solid hydrocarbon gel comprising: a) a solid or semi-solid hydrocarbon; and b) at least one block copolymer selected from the group consisting of: a triblock copolymer; a radial block copolymer; a multiblock copolymer; a diblock copolymer; and mixtures of these polymers. The hydrocarbon gel is useful as an ointment, balm or salve for wounds. Medicinal ingredients may be included in the hydrocarbon gel for application of such ingredients to wounds, burns or injuries.
CN102600349A Health-promoting composition and its application The invention discloses a health-promoting composition which mainly comprises (by weight parts) Ophiopogon japonicus polysaccharide 30-98, composite vitamins 1-50, and composite minerals 1-50. The composition can be made into any common oral preparation. The invention also discloses application of the composition in preparing health products for lowering blood sugar, improving insulin resistance, and recovering physical function. The composition provided by the invention has effects of lowering blood sugar, improving insulin resistance, supplementing vitamins and minerals for diabetes patients, and recovering physical function for patients.
CN103520243A Cyclic adenosine monophosphate snow chrysanthemum oil resin composite soft capsule and preparation method thereof The invention discloses a cyclic adenosine monophosphate snow chrysanthemum oil resin composite soft capsule and a preparation method thereof. The purity of cyclic adenosine monophosphate prepared by taking a Xinjiang Kunlun snow chrysanthemum oil resin which is prepared by extracting carbon dioxide in a supercritical mode and red date cyclic adenosine monophosphate which is prepared through reverse phase silica gel chromatography as base effective components, and by adopting a cAMP crude product which is prepared by purifying reverse phase silica gel, is 44.69%; the Xinjiang Kunlun snow chrysanthemum oil resin is prepared from carbon dioxide in a supercritical extraction mode, the snow chrysanthemum oil resin is taken as a medium, soyabean lecithin is added as an emulsifying agent, beewax is added as a suspending agent, the ratio of the cyclic adenosine monophosphate to the snow chrysanthemum oil resin is 1:6.5, 12% of cyclic adenosine monophosphate powder, 78% of the snow chrysanthemum oil resin, 5% of the beewax and 4% of the soyabean lecithin are adopted, and the cyclic adenosine monophosphate snow chrysanthemum oil resin composite soft capsule which is prepared through blending the raw materials not only has the advantages of safety, no toxicity, stable quality and the like, but also has health-care functions of blood pressure reduction, oxidation resistance and the like, and good antisepsis and anti-inflammation function, and has wide application values.
EP2292242A1 A scutellarin derivative, the preparing process, the pharmaceutical composition and the use thereof A scutellarin derivative, 4',5,6- trimethoxy-7-hydroxy-flavon-O-(2,3,4-tri-O-acetyl-glucuronide), the preparing process, the pharmaceutical composition and the use thereof are provided. The compound is obtained by methyl-etherification and acetylation of scutellarin as staring material and then separation. The compound of the present invention and the pharmaceutical composition thereof can be used for treating cardio-cerebro vascular diseases, inflammation and tumor.
CN1861591A Hesperetin derivant and preparation process thereof A hesperetin derivative with high anti-inflammatory activity and its preparing process are disclosed.
WO2005069771A3 Small molecule antagonists of bcl-2 family proteins The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the nati-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2 Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotheratpeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.
WO2010024405A1 Ifn type-1 production inhibitor and method for searching for same It is found that Spi-B can act cooperatively with IRF-7 to induce the production of IFN type-I. Based on this finding, it becomes possible to provide: an IFN type-I production inhibitor comprising an antisense nucleic acid or siRNA for Spi-B or an expression vector capable of expressing the antisense nucleic acid or the siRNA; a method for searching for a substance capable of inhibiting the production of IFN type-I, which comprises selecting a substance that inhibits the expression or function of Spi-B as the substance capable of inhibiting the production of IFN type-I; an IFN type-I production inducer comprising a combination of an expression vector capable of expressing Spi-B and an expression vector capable of expressing IRF-7; and others.
WO2012087181A1 Pharmaceutical composition for treating viral diseases The invention relates to medicine, and specifically to medicinal preparations on the basis of peptides. The composition comprises 0.01 - 0.03 mg per therapeutic dose of an inducer of endogenous interferon - a dipeptide of glutamic acid, selected from the group consisting of alpha-glutamyl tryptophan, gamma glutamyl tryptophan and alpha-lysyl glutamine. The composition also comprises a co-inducer of endogenous interferon - glycyrrhizic acid, taken in the form of a sodium salt or ammonium salt in an amount of 50 - 500 mg per dose.
WO2007089030A1 Use of 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or salt thereof for treating retrovirus infection The present invention provides a use of a therapeutically effective amount of 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (herein referred to as Compound I) or a pharmaceutically acceptable salt thereof, for the production of an agent for the treatment in a patient. The invention further provides a use of Compound I or a salt thereof for an agent for inhibition of integrase activity. Compound I or a salt thereof is also effective in inhibiting the replication of a retrovirus resistant to at least one anti-retroviral drug. In the use of the invention, Compound I or a salt thereof may be administered alone or in combination with at least one anti-retroviral drug other than Compound I or a salt thereof. The present invention also provides kits comprising Compound I or a salt thereof.
EP2300000A1 Methods and compositions for reducing inflammation and treating inflammatory disorders Methods of treating an inflammatory disorder and inhibiting inflammation by administering an inhibitor of a pH-activated protease are provided.
CN101775059A Novel glycyrrhetinic acid derivative, and preparation method and medicinal uses thereof The invention discloses a novel glycyrrhetinic acid derivative, and a preparation method and medicinal uses thereof. The glycyrrhetinic acid derivative is a compound prepared by coupling nitric oxide donor of furazan nitrogen oxides and glycyrrhetinic acid through ester bonds or amide bonds. As proved by pharmacological experiments, the glycyrrhetinic acid derivative has superior antitumor effectand can be used for the preparation of antitumor medicines.
CA2580919A1 Gastric inhibitory polypeptide (gip) antigen arrays and uses thereof The present invention is in the fields of medicine, public health, immunology, molecular biology and virology. The present invention provides, inter alia, a composition comprising a virus-like particle (VLP) and at least one antigen, wherein said antigen is a GIP protein or a GIP fragment linked to the VLP respectively. The invention also provides a method for producing the aforesaid composition. The compositions of this invention are useful in the production of vaccines, in particular, for the prevention and/or treatment of obesity and hereby, in particular, by inducing efficient immune responses, in particular antibody responses. Furthermore, the compositions of the invention are particularly useful to efficiently induce self-specific immune responses within the indicated context.
EP1501836A1 Halo-alkyl esters of camptothecins and methods of treating cancer using these compounds Halo-alkyl esters of camptothecin are described. Processes for making these compounds and for using them in cancer treatment, are also described.
US20080085314 Comprises controlled release acetaminophen, non-steroidal anti-inflammatory drug, and agent capable of reducing gastric acid secretion A first, solid oral pharmaceutical composition includes an extended release acetaminophen, a non-steroidal anti-inflammatory drug, such as naproxen or ibuprofen, and a third drug capable of reducing gastric acid secretion, such as ranitidine or omeprazole. A second, solid oral pharmaceutical composition includes a non-steroidal anti-inflammatory drug and an agent for reducing gastric acid secretion.
WO2011123623A3 Skin, nail and hair topical antimicrobial methods using formulations containing organosilane quaternaries A method for treating human or animal skin, hands, feet, hair or nails to eliminate or reduce the number of microorganisms thereon by topical application of an aqueous formulation comprising antimicrobial organosilane quaternary ammonium compounds and benzalkonium chloride of the quaternary group, which provides antimicrobial and antiseptic activity. The method prevents reinfection for at least 12, preferably 24 and most preferably at least 60 hours. The formulation may further comprise methyl anthranilate, which performs the dual functions of fragrance (grape fragrance) and biocidal agent. The formulation may further comprise other compatible inert but desirable ingredients such as moisturizers, color and fragrance.
EP1309590B1 Azaindole derivatives, process for their preparation, and their use as antitumor agents Novel 1H-pyrrolo[2,3-b]pyridines which are represented by formula (I), as per the specification, and wherein R is a hydrogen or halogen atom or a group selected from -CN, -OH, -OCOR4, -(CH2)nNH2, -(CH2)nNHR4, -(CH2)nNHCOR4, -(CH2)nNHCONR4R5, -(CH2)nNHCOOR4, or -(CH2)nNHSO2R4, wherein n is either 0 or 1, R4 and R5 are as described in the specification; R1 is hydrogen or an optionally substituted alkyl group; R¿2? is an optionally substituted group selected from alkyl or aryl; R3 is hydrogen or a group selected from -CONR4R5, -COOR4, -CONHOR4, -SO2NHR4, alkylsulphonylaminocarbonyl or perfluorinated alkylsulphonylaminocarbonyl; or a pharmaceutically acceptable salt thereof, are disclosed; these compounds are useful for treating cell proliferative disorders associated with an altered cell cycle dependent kinase activity.
CN101914095B 2-chloropyridine derivative, preparation method and application thereof to preparation of medicines resistant to liver cancer The invention discloses a 2-chloropyridine derivative which has the general formula as specification. In the formula, R is FORMULA. The 2-chloropyridine derivative has obvious inhibiting effect on the growth of the human liver cancer cells (Hep-G2). Therefore, the 2-chloropyridine derivative can be applicable for the preparation of medicines resistant to liver cancers. The invention discloses a preparation method of the 2-chloropyridine derivative.
US20080312209 Piperazine Heteroaryl Derivatives as Gpr38 Agonists The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Z, X and B are as defined in the specification. The compounds are partial or full agonists at the GPR38 receptor. Pharmaceutical compositions comprising the compounds, methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.
CN1879787A A hicismus-treating medicine with tulip The invention provides a medicament for treating body odor, which is prepared from the following raw materials (by weight ratio): tulip, buthus martensi karsch, camphor, malachite, perfume compound and ethanol. Its preparing process consists of the steps of disintegrating, sieving, mixing with ethanol and immersing in containers.
CN100594933C Antiobestic agents and health foods Antiobestic agents and health foods containing as the active ingredient substances having an effect of adsorbing bile acid in the digestive tract an effect of inhibiting intestinal circulation or an effect of inhibiting the absorption of exogenous lipids typified by pharmaceutically acceptable anion exchange resins. In particular, antiobestic agents and health foods characterized by lowering bodyweight and/or visceral fat content without reducing food intake.
CN103520707A Probiotic and bacteria-treating composition for preventing and treating infection of reproductive system The invention discloses a probiotic and bacteria-treating composition for preventing and treating infection of a reproductive system. The composition comprises the following components by weight percent: 5-9% of carbomer, 1-5% of tea tree oil, 0.0001-0.0009% of recombinant human epidermal growth factor, 0.8-4% of carotenoids extract, and 0.9% of balanced salt. By adopting the composition, the moisture content of dynamic cells in different environments can be effectively adjusted; the composition is free of thrill and sensitization response, and strong in adsorbability in mucosa; vaginal epithelial cells can be deeply nourished; premature ovarian failure is resisted; dropping of senescent cells and retro-differentiation into young cells are accelerated; growth of probiotics is facilitated; the composition has the effects of stopping bleeding, itching and pain and repairing a mucosal injury; balance of PH value of a vaginal microecosystem is effectively maintained; malignant bacteria, mycete, fungi and trichomonad can be inactivated; virus infection is inhibited; the elastic tension immunity and the self-purification function of the vagina are improved; a good repair environment is provided to an injured cell; the healing time of an ulcer wound is shortened; the healing quality is also improved.
WO2012112232A1 METHODS AND COMPOSITIONS FOR TREATING β-THALASSEMIA AND SICKLE CELL DISEASE The present invention provides compounds (such as compounds of formula I-a) that induce γ globin expression and pharmaceutical compositions thereof. Such compounds may have beneficial therapeutic effects. Compounds and compositions described herein may be used to treat hemoglobinopathies such as β-thalassemia and sickle cell anemia. (I-a)
EP2000137A9 Triglyceride-lowering agent and hyperinsulinism-ameliorating agent The present invention is directed to a triglyceride-lowering agent, exhibiting excellent triglyceride-lowering effect and a hyperinsulinemia-ameliorating agent. The triglyceride-lowering agent and hyperinsulinemia-ameliorating agent are characterized by containing a pitavastatin compound, and amlodipine or a salt thereof.
WO2014118229A1 Substituted thienopyrimidines and pharmaceutical use thereof The present invention relates to substituted thienopyrimidine compounds of general formula(I)as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
EP1286975B1 Biclyclic cyclohexylamines and their use as nmda receptor antagonists Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are defined in the specification.
US20130059901 Pre-MRNA Trans-Splicing Molecule (RTM) Molecules and Their Uses The present invention relates to specific and markedly improved pre-mRNA trans-splicing molecule (RTM) molecules which are designed to correct specific genes expressed within cells to be targeted, and which are associated with epidermolysis bullosa, cystic fibrosis, pachyonychia congenital, and psoriasis or neurodermitis, as well as cancers of the skin. In particular, the RTMs of the present invention are genetically engineered to interact with a specific target pre-mRNA expressed in cells to be targeted so as to result in correction of genetic defects or reprogramming of gene expression responsible for a variety of different skin disorders.
CN102176911A Novel adenine derivatives The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure: n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the -(CH2)n- moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
US20090023750 Novel salts of piperazine compounds as d3/d2 antagonists The present invention relates to novel monohydrochloride, dihydrochloride, monohydrobromide, maleate and methanesulphonate salts of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention relates to the process for preparing the salts and their hydrates and/or solvates, to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to pharmaceutical compositions containing them.
US20080027010 Treatment of refractory cancers using Na+/K+-ATPase inhibitors The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach to treat refractory cancers using Na+/K+-ATPase inhibitors, such as cardiac glycosides, including bufadienolides or their corresponding aglycones (e.g., proscillaridin, scillaren, and scillarenin, etc.), especially in oral formulations and/or solid dosage forms containing more than 1 mg of active ingredients.
CN1911244A Slow-released type iron-complement agent, prepn. method and use thereof A slow-release Fe supplement used as the Fe-supplementing additive of forage or to prepare Fe-supplementing food or medicine for treating diseases is a cationic exchange resin containing the active Fe. It is prepared through the ionic exchange between 2-valence Fe salt and anionic exchange resin, filtering, drying and pulverizing.
CN103319479A Rheinic acid berberine ion pair compound, preparation method and applications The invention relates to a rheinic acid berberine ion pair compound with a formula (I) structure and a preparation method thereof, comprising the following steps of: (1) preparing a berberine hydrochloride solution, (2) adding rheinic acid or an alkali metal salt of rheinic acid into the solution obtained in the step (1), heating, stirring and fully reacting; and (3) filtering, washing, refining and drying the reaction products to obtain the rheinic acid berberine ion pair compound. The invention further relates to pharmaceutical compositions containing the ion pair compound, wherein the weight of the ion pair compound is 0.1-99.9% that of the compositions. The invention also relates to applications of the ion pair compound and the compositions thereof for preparing medicines for treating bacterial infection, peptic ulcer, diabetes, hyperlipemia, obesity, arthritis, heart failure, arrhythmia, platelet aggregation, hypertension, intestinal adhesion, etc. The rheinic acid berberine ion pair compound can increases lipid solubility of rheinic acid and berberine, and substantially raises a biological utilization degree.
US20110190285 Methods of treating a botulinum toxin related condition in a subject The present invention provides methods of treating a botulinum toxin related condition in a subject. In certain embodiments, the methods involve administering a compound of the following formulas: (I), (II), (III), (IV), (V).
WO2007053807A2 Calcitriol for treating intraocular diseases associated with angiogenesis The present invention provides a method of treating pathologies resulting from neovascular growth in the eye such as those manifested as retinopathy of prematurity, diabetic retinopathy and macular degeneration. The invention comprises the administration of an effective amount of calcitriol that is administered at doses less than toxicity and results in a significant reduction in the formation of neo-vascular growth. The invention can be used to treat existing diseases or prophylactically to treat those at risk.
WO2006041888A3 Substituted aryl or heteroarylsulfonylbutanamides for use as anti-inflammatory agents Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
WO2008043829A2 Method for treating hiv-1 infection by the combined administration of nevirapine, tenofovir and emtricitabine The invention provides a method for treating HIV wherein emtricitabine, tenofovir and nevirapine are administered once per day.
CN102512430A Medicinal composition for intestinal tract cleaning The invention discloses a medicine for colonoscopy and intestine tract preparation before colonic and rectal surgeries. The medicine is a medicinal combination containing L-glucose and L-mannose. The L-glucose and the L-mannose are not required to be separated, so the production cost is reduced; and the method has high industrial value. The medicinal combination of the L-glucose and the L-mannose has the characteristics of safety, reliability, convenience for use, good patient compliance and the like.
CN101199534B Anti-tumor function of raw panoxadiol derivative The invention discloses a compound 25hdt of protopanaxadiol derivative, that is, 20 ( R ) -25- hydroxy-dammarane type-3- Beta, 12 Beta, 20-triol, for preparing anti-cancer drugs. The compound 25hdt better inhibits tumor cell lines outside the human than PPD, ginsenoside- Rg3 and Rh2. At the same time, the compound 25hdt inhibits the tumor cells of the human from regulating, induces the tumor cells of the human to be apoptotic, inhibits the tumor cells of the human from proliferating and specifically inhibits the tumor cells of the human from growing. When the compound 25hdt is used to treatthe cancers, the compound 25hdt does not cause the obvious changes of the weight of the experimental animal without any other toxic effect. Matched with other embolic chemotherapy or radiation methods to treat the cancers, the compound 25hdt can better improve the efficacy.
CN101040851A The use of dicaffeoylguinic acid ramification and the analog in the treatment of diabetes and the corresponding disease The invention relates to the application of 2-caffeoyl guinic acid and relative derivant in the treatment of diabetes or the like.
US7008637 Transdermally administered tolterodine as anti-muscarinic agent for the treatment of overactive bladder The present invention is drawn to set of formulations of at least one compound selected from tolterodine, salts thereof, prodrugs thereof and/or metabolites thereof, wherein in the set of formulations contains at least one device for transdermal administration and at least one formulation for oral, sublingual, buccal, nasal, pulmonary, rectal and/or other transmucosal administration, in order to achieve an effect against overactive bladder and/or symptoms associated with this condition. The present invention is further drawn to methods of treating an overactive bladder with the formulations.
CN101180044B Combination of EGF/GHRP-6 for neuroregeneration of central nervous system The invention is intended to simulate neuroregeneration of the central nervous system following autoimmune damage. More specifically, the invention relates to the pharmaceutical combination comprising therapeutically-effective concentrations of epidermal growth factor and human growth hormone secretagogue hexapeptide, which is administered to a patient suffering from the symptoms of multiple sclerosis and neuromyelitis optica and which corrects demyelination caused by autoreactive cells in the central nervous system.
WO2013170985A1 New aminoglycoside antibiotics targeting bacterial 16s ribosomal rna lacking ototoxicity The present invention relates to paromamine-/neamine-based compounds according to formula I or II having selective antimicrobial activity directed at ribosomal 16S RNA and lacking ototoxicity. Furthermore, the invention is directed to the use of said compounds for preparing a medicament, pharmaceutical preparations, and methods for preparing said compounds.
CA2289017C The use of a nitroxide or a prodrug thereof in the prophylactic and therapeutic treatment of cancer The present invention provides a method for the prophylactic and therapeutic treatment of cancer. The method comprises administering to an animal, preferably a mammal, more preferably a human, at risk for developing a cancer or having a cancer a nitroxide or a prodrug thereof, wherein the nitroxide or prodrug thereof preferably is alicyclic or heterocyclic and more preferably is a compound of Formula (I) or Formula (II): in an amount sufficient to prevent or treat said cancer, wherein said cancer is susceptible to prevention or treatment by said nitroxide or prodrug thereof. Also provided is a composition for use in the method.
DE102007043177A1 Use of a composition containing an ingredient e.g. hydrated silicic acid, sorbitol, glycerin, polyethylene glycol, sodium lauryl sulfate, sodium fluoride, titanium dioxide, xanthan and carrageen for the treatment of hematoma Use of a composition containing at least an ingredient, which is hydrated silicic acid, sorbitol, glycerin, polyethylene glycol, sodium lauryl sulfate, sodium fluoride, titanium dioxide, xanthan, carrageen, sodium saccharin, lime, 6-chloro-2-(6-chloro-4-methyl-3-oxo-benzo[b]t hiene-2(3H)-ylidene)-4-methyl benzo[b]thiophene-3(2H)-one, [29H,31H-phthalocyaninato(2-)-N-(29)-,N-(30)-,N-(31)-,N-(32)-]copper, camomile, sage, eucalyptus, peppermint, myrrh and/or star anise, for the treatment of hematoma, is claimed. - ACTIVITY : Antianemic. - MECHANISM OF ACTION : None given.
US20110183912 Agent for promoting neuronal differentiation and method therefor An agent for promoting neuronal differentiation of a neural stem/progenitor cell includes an inhibitor of function of a COUP-TFI protein and/or a COUP-TFII protein. To promote neuronal differentiation of a neural stem/progenitor cell, the agent is administered to the neural stem/progenitor cell to inhibit function of a COUP-TFI protein and/or a COUP-TFII protein.
WO2014076135A1 Bpo wash gel composition The present invention relates to a topical dermatological/pharmaceutical composition comprising BPO wherein the composition is a wash composition with desirable tolerance, stability and foaming properties. The composition comprises: a) Benzoyl peroxide (BPO), b) At least one mild surfactant selected from anionic and/or non-ionic surfactant classes, c) Zinc gluconate, d) Dipotassium glycyrrhizate, e) At least one gelling agent. The composition is preferably in the form of an aqueous gel or an aqueous-alcoholic gel. The invention also concerns the use of such composition for the treatment of dermatological disorders, and in particular in the treatment of acne.
CN102600099A Method for preparing sinomenine hydrochloride sustained release tablets by non-organic solvents The invention discloses a method for preparing sinomenine hydrochloride sustained release tablets, in particular to a method for preparing sinomenine hydrochloride sustained release tablets by non-organic solvents. In the method, conventional highly toxic benzene extraction and chloroform extraction (solvent extraction) processes are replaced by cation exchange resin or macroporous resin adsorption, the extraction yield is high, the operation is easier, harms and pollution caused by large organic solvent dosage and large toxicity to the health of operators and the environment are overcome, the treating processes of organic solvents are reduced to be conductive to environment protection and environment-friendly production, and the investment in environmental protection facilities of plantsis reduced. The sinomenine hydrochloride extracted and separated by the method disclosed by the invention is used as the raw material of pharmaceutical preparation, and has higher purity without solvent residue, and potential hazards to the human body are reduced.
CN101352436A Novel medicament composition for resisting thrombosis The invention relates to a medical composition, in particular to a novel antithrombotic medical composition and a preparation method and a purpose thereof. The novel antithrombotic medical composition comprises ADP receptor antagonist with an effective dose of 25-500mg and Indobufen with an effective dose of 50-400mg. The invention reduces the spread effect to gastrointestinal tract and the severe bleeding probability that appears in the application of ticlopidine-aspirin composition and Clopidogrel-aspirin medical composition, more particularly reduces the bleeding incidence rate of the gastrointestinal tract, improves the medication compliance of patients and the clinical medication safety and healing efficiency and has favorable using value.
WO2013071061A1 Compositions and methods for increasing stress resilience Compositions and methods for increasing resilience to the effects of stress are provided. Methods inhibit, treat, and/or prevent a stress- related disorder or symptoms thereof are provided. The method comprises increasing sphingosine-1 -phosphate receptor 3 (SIP3 receptor) expression and/or activity. The method comprises administering to a subject at least one SIP3 receptor encoding nucleic acid or SIP3 agonist.
US7534859 Protein kinase C epsilon as modulator of anxiety, alcohol consumption and self-administration of drugs of abuse The present invention is directed to the production of PKC isozyme ε (PKCε)-deficient cells and non-human animals. The present invention is further directed to the identification of PKCε as a target for drugs that reduce anxiety. According to the present invention, PKCε-inhibiting compounds act in synergy with drugs acting at the GABAA receptor. The present invention is also directed to the use of modulators of PKCε to modulate alcohol consumption, self-administration of other drugs of abuse, and the effects of alcohol consumption as well as the use of inhibitors of PKCε, either alone or in conjunction with allosteric agonists of GABAA receptors, to treat conditions, such as addiction, withdrawal syndrome, skeletal muscle spasms, convulsive seizures, and epilepsy, that are amenable to treatment by allosteric agonists of GABAA receptors. Additional aspects of the present invention are diagnostic methods for identifying individuals at risk for becoming alcoholics or abusers of other drugs and kits for performing such diagnostic methods. The present invention relates to: cells and non-human animals deficient for the PKC isozyme ε (PKCε); the use of PKCε as a target for drugs; the use of inhibitors of PKCε in methods of reducing anxiety and treating conditions associated with insufficient activity of the GABAA receptor; the use of modulators of PKCε in methods of modulating alcohol consumption, modulating self-administration of other drugs of abuse, and altering the effects of alcohol; pharmaceutical compositions comprising inhibitors of PKCε and allosteric agonists of GABAA receptors; and the identification of individuals with enhanced susceptibility to alcoholism or other forms of addiction.
CA2574308C Benzyltriazolone compounds as non-nucleoside reverse transcriptase inhibitors The present invention relates to a compounds according to formula (I), methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula (I) and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula where R1, R2, R3, R4, R5, are as defined herein.
US7176276 Antimicrobial peptide and use thereof An object of the invention is to provide an antimicrobial peptide having an amino acid sequence which is different from a peptide existing and functioning as an antimicrobial peptide in the natural world and is not based on the conventional developmental approach for an antimicrobial peptide-containing antimicrobial agent, and a polynucleotide coding for said peptide. Another object is to provide an antimicrobial agent which contains such an antimicrobial peptide. Namely, an antimicrobial peptide represented by a general formula (1) (Xa)n-S (1) wherein Xa of the formula (1) is a hydrophilic amino acid residue, n is an integer of from 1 to 6, two or more of the Xa may be the same or different from one another, S is a peptide represented by hydrophobic amino acid part-basic amino acid part-bridge part-basic amino acid part-hydrophobic amino acid part, and amino acid residue of the bridge part is selected from the group consisting of hydrophobic amino acids and neutral amino acids.
CN100998558A Slow-release anticarcinogen contg. carmustine and fluorouracil A slow-release anticancer medicine in the form of injection or implant contains carmustine and its synergist chosen from 5-FU, cisplatin and 06-benzylguanine. For said slow-release injection, it is composed of the slow-release microballs containing the active anticancer component and slow-releasing auxiliary and the special solvent containing suspending aid.
CN102824347A Application of securinine in preparing medicine for suppressing MDA-MB-157 cell proliferation The invention discloses application of securinine in preparing a medicine for suppressing MDA-MB-157 cell proliferation. The Chinese name of securinine is also called 'Yeqiujian' and 'Xiaosuanyeqiujian'. The chemical name is (6S,11aR,11bS)-9,10,11,11a-tetrahydro-8H-6,11b-methyl furano-[2,3-c]pyridino-[1,2-a]azepine-2(6H)-ketone; and the securinine can suppress the MDA-MB-157 cell proliferation according to the current discovery.
US20120107401 Osteoconductive matrices comprising statins and methods of using the same Osteoconductive matrices and methods are provided that have one or more statins disposed therein. The matrices may be injected into a fracture site. The osteoconductive matrices provided allow for sustain release of the statin and facilitate bone formation and repair of the fracture site.
US6960602 Piperidine derivatives as modulators of chemokine receptors The invention provides a compound of formula (I): wherein R1, R2, R3, R3a, R4, R4a, R5, and R6 are as defined; or a pharmaceutically acceptable salt thereof or a solvate thereof; compositions containing these compounds, processes for preparing them and their use as modulators of chemokine activity (especially CCR5 activity)
CN1876077A A medicament for treating superficial lymphoid tuberculosis The invention relates to a medicament for the treatment of superficial lymph gland tuberculosis, which comprises adhesive plaster and pellets and has the advantages of short course of treatment and low treating cost.
WO2013116786A1 Cdk8/cdk19 selective inhibitors and their use in anti-metastatic and chemopreventative methods for cancer The invention relates to the compounds and methods for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds and methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI -related diseases. The invention provides new compounds having improved solubility and/or potency, and methods for their use. In various aspects, the invention relates to the treatment of cancer. The invention provides methods for chemoprevention and prevention of tumor recurrence or metastasis. The invention further provides diagnostic techniques for treatment for certain cancer types. The invention utilizes specific inhibitors of CDK8/19 and/or measurement of CDK8 levels in a patient.
CN1726915A Nasal cavity taken drug system and combination of naloxone hydrochloride and preparation method A nasal application system or composition of naloxone hydrochloride contains the naloxone hydrochloride or its free alkali or its other medicinal salts, absorption promoter, osmotic pressure regulator, antiseptic, and solvent or other medicinal auxiliaries. Its preparing process s also disclosed.
US20090156525 Low-Density Lipoprotein Receptor-Related Protein 2 Clears Amyloid-Beta Peptide A cross the Blood-Brain Barrier via Apolipoprotein J Low-density lipoprotein receptor-related protein 2 (LRP2) is a potential receptor to regulate the level of apolipoprotein J (apoJ) in the central nervous system, which is the major carrier of amyloid-β peptide (Aβ). ApoJ is cleared from brain interstitial fluid (ISF) and cerebrospinal fluid (CSF) by LRP2-mediated transcytosis across epithelial and endothelial barriers. At physiological ISF/CSF levels, apoJ is rapidly transported by LRP2 across the blood-brain barrier (BBB). Importantly, apoJ also substantially enhances clearance from the brain of amyloidogenic Aβ isoforms (i.e., higher β-sheet content such as Aβ42) as apoJ-Aβ by LRP2-mediated transport.
CN101903027A Preventive or therapeutic agent for inflammatory bowel disease The invention relates to a pharmaceutical composition for preventing or treating an inflammatory bowel disease comprising 7,8-dimethoxy-4(5H),10-dioxo-1H-1,2,3-triazolo[4,5-c][1]benzoazepine, a prodrug thereof, preferably 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzoazepine as the prodrug, or a pharmacologically acceptable salt thereof. The pharmaceutical composition according to the invention is effective in the prevention and treatment of an inflammatory bowel disease and has few side effects. In particular, the pharmaceutical composition according to the invention can exhibit a potent preventive effect and therapeutic effect also on a severe case showing resistance to existing therapeutic agents.
US20120122830 Pregnenolone sulfate for the treatment of neurologic disorders The disclosure relates, in part, to methods of using pregnenolone sulfate (PREGS) to protect against the neurotoxicity of the β-amyloid peptide Aβ1-42. The disclosure also provides methods of using pegnanolone sulfate for treating neurologic disease or dysfunction. The disclosure further provides of using pegnanolone sulfate methods for stimulating or promoting growth of a neuronal cell.
US20090176864 Methods For Improving Hepatic and Immune Function In An Animal The invention encompasses compositions and methods for improving animal health and in certain embodiments to compositions and methods for improving hepatic and immune function in aged felines.
CN1903185A Dispersion tablets and its prepn. method A dispersing tablet contains proportionally L-glutamine, sodium azulenesulfonate, and additives including disintegrant. Its preparing process is also disclosed.
US20120321673 Transdermal drug delivery system and method of using the same A transdermal drug delivery system comprising a steroid as an active agent, wherein the steroid may be clobetasol propionate, betamethasone dipropionate, amcinonide, or loteprednol etabonate. The transdermal drug delivery system also comprises a pressure-sensitive adhesive layer and a support, wherein the steroid is present in the pressure-sensitive adhesive layer, and wherein the pressure-sensitive adhesive layer is provided on a support. The transdermal drug delivery system may be applied onto the eyelid of a patient in need thereof, in order to treat a disease of the eyelid, such as chalazion, blepharitis or meibomian gland dysfunction.
CN103664991A Thiophene [2, 3-d] pyrimidine derivative as well as preparation method and use thereof The invention provides a thiophene [2, 3-d] pyrimidine derivative containing isoxazole heterocycle shown by formula (I) or a pharmaceutically accepted salt thereof, wherein R1 and R2 are respectively selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, aryl optionally substituted by R<7> or heteroaryl optionally substituted by R<8>; or R1, R2 and carbon atoms connected with R1 and R2 form 4-membered to 6-membered carbocycle or heterocycle; Z is -NR5-, C(R6)2, -S- or -O-; R3 is selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, halogenated C1-6 alkyl or halogenated C1-6 alkoxy; n is an integer from 0 to 5; R4 is selected from hydrogen, C1-6 alkyl, c1-6 alkoxy, halogenated C1-6 alkyl, aryl optionally substituted by R<9> or heteroaryl optionally substituted by R<10>. The invention further provides a preparation method and medical use of the compound represented by the formula (I) as well as the pharmaceutically accepted salt thereof; the compound can act as a medicine or a lead compound for treating tumor, cancer and other diseases.
EP1560581A1 Oromucosal formulation and process for preparing the same An oromucosal formulation comprising as an active ingredient a substituted imidazole derivative of formula (I) [please enter chemical formula here] where Y is -CH2- or -CO-, R1 is halogen or hydroxy, R2 is H or halogen and R3 is H or lower alkyl, or an acid addition salt thereof, together with additives conventionally used in oromucosal formulations, and a process for its preparation.
US20100062082 Ion sensor for fluid and method for its manufacture The invention provides a method for the measurement of a concentration of a charged species in a sample, the sample having a plurality of types of charged species and at least one insoluble component. The method comprises: providing the sample on a surface of a partly permeable layer (30); allowing components of the sample to pass through the partly permeable layer (30) into a channel (12); and separating the components into sections, such that each at least one of the sections substantially comprises a single type of the plurality of the types of charged species, and determining the charge concentration in the at least one of the sections.
US20080033009 Solid Pharmaceutical Formulation This invention provides a solid pharmaceutical formulation having high physical strength and further having excellent drug release properties and digestibility of excipients when administered, which comprises (a) an active medical ingredient and (b) a pre-gelatinized starch in an amount of 10 to 90% by weight, said pre-gelatinized starch being prepared by pre-gelatinizing a cheap and stable usual starch during the procedure for formulation. This invention also provides a method for preparing the solid pharmaceutical formulation.
US7393830 Prolactin induced increase in neural stem cell numbers The present invention provides a method of increasing neural stem cell numbers or neurogenesis by using prolactin. The method can be practiced in vivo to obtain more neural stem cells in situ, which can in turn produce more neurons or glial cells to compensate for lost or dysfunctional neural cells. The method can also be practiced in vitro to produce a large number of neural stem cells in culture. The cultured stem cells can be used, for example, for transplantation treatment of patients or animals suffering from neurodegenerative diseases or conditions. In addition, since neural stem cells are a source for olfactory neurons, the present invention also provides methods of increasing olfactory neurons and enhancing olfactory functions.
EP1135117B1 Medikament for treating chronic obstructive pulmonary disease A class of OMEGA -substituted(1,4-benzoquinon-2-yl)alkanoic acids are useful in the treatment of chronic obstructive pulmonary disease (COPD). The preferred compound for the method of treatment is 7-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-7-phenylheptanoic acid or a pharmaceutically acceptable salt, ester or pro-drug thereof.
WO2007091948A3 Novel spiro [imidazolidine-4, 3´-indole] 2, 2´,5´(1h) triones for treatment of conditions associated with vanilloid receptor 1 The present invention relates to new compounds of formula (I), wherein R1 to R9 and X are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
EP2777713A1 Polyethylene glycol-amino acid oligopeptide-irinotecan drug conjugate and drug composition thereof A PEG-oligopeptide-irinotecan conjugate with a general formula (I) and the pharmaceutical composition comprising the conjugate are disclosed. In the conjugate, PEG represents polyethylene glycol with a molecular weight of 300-60,000 Daltons; (AA)i represents an oligopeptide, AA represents the same or different amino acids in the oligopeptide; i is an integer of 2-12 representing the number of amino acids in oligopeptide; j is an integer of 2-12 representing the number of irinotecan connected with the oligopeptide. In the conjugate, each terminal group of PEG can link with multiple irinotecans through oligopeptides, thereby greatly increasing the drug-loading capacity. Modification of the hydrophilic polymer can provide protection for the irinotecan, thereby improving drug absorption, prolonging the action time, enhancing the efficacy, reducing the dose and avoiding the toxic and side-effects.
WO2013158649A1 Compositions and methods of modulating 15-pgdh activity Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.
US20100227935 Class of terpene-derived compounds having an antibiotic activity, compositions containing the same and uses thereof The present invention relates to a new class of terpene-derived compounds having an antibiotic activity and of the formulae (I) or (II) in which A is selected from NR1, O, S, CR2R3 or R—(CH2)n—R′, wherein R and R′ represent independently NH, O, S or CH2, and in which R1, R2 et R3 are substituents and n is higher than or equal to 1, in particular equal to 2. The invention relates to the compound according to both the formula (I) or the formula (II) taken individually, to mixtures of the two compounds, and to compositions, mainly therapeutic ones, comprising at least one of the compounds or said mixture. According to a particular embodiment, the compound ((I) or (II) taken individually, the mixtures of both compounds and the compositions of the invention are used in the treatment of difficult C-related digestive infections. In one particular embodiment, the compound of the formula (I) is margaucine, a compound produced by a bacterial stem.
CN103446077A Salbutamol sulfate oral instant membrane and preparation method thereof The invention relates to an oral instant membrane containing salbutamol sulfate. The instant membrane comprises the following raw materials by weight: 1-4 parts of salbutamol sulfate, 5-20 parts of hydroxypropyl methyl cellulose, 0.1-4 parts of modified starch, 1-10 parts of microcrystalline cellulose, 0.1-4 parts of poloxamer, 1-4 parts of silica, 0.1-4 parts of Simethicone, 0.1-4 parts of polyethylene glycol 400, 0.01-1 part of sucralose and 0.1-4 parts of essence. The salbutamol sulfate membrane provided by the invention does not require water for administration, and can disperse rapidly (equal to an oral solution) if being put on the tongue surface and go into the stomach with saliva, and does not need a disintegration process after oral administration; therefore, the salbutamol sulfate oral instant membrane has the characteristics of fast absorption, fast effectiveness and high degree of bioavailability, can be applied to alleviation of acute bronchus spasm, long-term maintenance and prevention therapy, and prevention of exercise-induced asthma.
US20110052593 Breast cancer associated antigen The invention relates to nucleic acid and amino acid sequences encoding BUC11 (SEQ ID NO: 36), BUC6 (SEQ ID NO: 31), BUC9 (SEQ ID NO: 32), and BUC10 (SEQ ID NO: 35), and to the use of such sequences in the identification and treatment of cancers.
WO2005030758A1 Pyrimidine and pyridine derivatives useful as hmg-coa reductase inhibitors and method of preparation thereof Compounds are provided having the following structure which are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hormone replacement therapy, hypercholsterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis identified in Formula (I) wherein X is N or CR5; and pharmaceutically acceptable salts thereof, Z is identified in Formula (II) or in Formula (III) ; wherein R1 to R7 are as defined herein. A method for treating the above diseases employing the above compounds is also provided.
CN101683349A Compound florfenicol powder for treating mycoplasma of pigeon and preparation method thereof The invention discloses a compound florfenicol powder for treating mycoplasma of pigeon and a preparation method thereof, and the objective of the invention is to provide a compound florfenicol powder, which has instant effect for treating ycoplasma of pigeon and has effect for secondary infection of bacteria, and a preparation method which is simple and easy to be realized. Florfenicol in powderis 2-10 wt%, oxytetracycline is 2-12%, atropine sulfate is 0.05-0.5%, doxofylline 0.2-1.5%, and the rest is anhydrous dextrose. Florfenicol and oxytetracycline kill pathogen, which reduces probabilityof drug tolerance; atropine sulfate controls secretion of the digestive tract gland; doxofylline suppresses cough and calms panting. The four ingredients use together has a combination and cooperation function, and can quickly treat disease against clinical symptoms of mycoplasma disease of pigeon and accelerate recovery of pigeon, and has the efficacies for seeking both temporary and permanent solution, simultaneously preventing and treating other bacteria secondary infections, reducing drug tolerance probability, and considerably improving cure rate.
US20100016433 Nerve-regenerating agent A nerve-regenerating agent comprising, as an active ingredient, arachidonic acid and/or a compound containing arachidonic acid as a constituent fatty acid.
EP2679584A1 Clathrate complex of cyclodextrin or arabinogalactan with 9-phenyl-sym-octahydroselenoxanthene The invention relates to novel clathrate complexes of cyclodextrin or arabinogalactan with 9-phenyl-sym-octahydroselenoxanthene, possibly in α-crystalline form, with a mass ratio of 9-phenyl-sym-octahydroselenoxanthene:cyclodextrin of from 1:3 to 1:30 or 9-phenyl-sym-octahydroselenoxanthene:arabinogalactan of from 1:10 to 1:20. The clathrate complex may be in crystalline form, possibly in the form of nano-particles with a size of less than 100 nm. In the clathrate complex, cyclodextrin is selected from α-, β-, γ- or hydroxypropyl-β-cyclodextrin, primarily β-cyclodextrin. The proposed clathrate complexes make it possible to increase the water-solubility of the active compound, to improve the bioavailability, to reduce the dosage of the drug and, consequently, to reduce the toxic effect of 9-phenyl-sym-octahydroselenoxanthene. The complexes exhibit cytoradioprotective activity. The invention also relates to a liquid-phase and solid-phase methods for producing clathrate complexes, as well as to pharmaceutical compositions and drugs thereof.
CA2758948A1 Method for the induction of a reward response by modulation of dopaminergic systems in the central nervous system A method of modulating the dopaminergic system of the central nervous system comprising administering to a subject a dopamine precursor and/or a dopamine agonist in an amount effective to induce a reward response in the subject is described, as are related composi-tions.
US20100247673 Thyroid protection in sickle cell anemia treatment In a method of providing anti-sickling of red blood cells in sickle cell anemia patients without hemolyzing the cells comprising, administering in a pharmaceutically acceptable vehicle an anti-sickling, non-hemolyzing amount of thiocyanate selected from the group consisting of alkali metal salts and an ammonium salt until the Hbss relative solubility ratio is at least 1.200 in the deoxygenated hemoglobin-S, the improvement of protecting the thyroid gland in the event of thiocyanate overdose, comprising administering along with the thiocyanate in the pharmaceutically acceptable vehicle, iodine in an amount sufficient to prevent thiocyanate overdose.
WO2011068208A1 Therapeutic agent for spinal and bulbar muscular atrophy Disclosed is a novel treatment strategy for spinal and bulbar muscular atrophy (SBMA). Specifically disclosed is a therapeutic agent for spinal and bulbar muscular atrophy, which comprises triptan or a pharmacologically acceptable salt thereof as an active ingredient.
US20090142300 Compositions and methods related to toll-like receptor-3 The invention relates to compositions and methods related to Toll-like receptor (TLR) polypeptides. In some embodiments, the invention relates to managing TLR3 related diseases. In further embodiments, the invention relates to methods of preventing and treating inflammation. In some embodiments, the invention relates to antagonists of TLR3, to amino acid sequences that act as dominant negative molecules, and to nucleic acid sequences that encode said amino acid sequences. In additional embodiments, the invention relates to the manipulation of biological materials to evaluate TLR3 activity.
US20120196928 Red yeast rice extract high in monacolin k content Compositions comprising Red Yeast Rice extracts which comprise greater than 5 wt. % monacolin K are useful for lowering cholesterol and/or triglyceride levels in a subject.
WO2014100734A1 Prmt5 inhibitors and uses thereof Described herein are compounds of formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
CN103450163A Indazole compounds, preparation method, and pharmaceutical applications thereof The invention firstly discloses a series of indazole compounds or physiology-acceptable derivatives thereof, a preparation method, and pharmaceutical applications thereof. The indazole compounds or physiology-acceptable derivatives thereof have the functions of inhibiting Rho kinase activity, relaxing blood vessels, protecting the functions of the blood vessels, protecting cardiac muscle cells from hypoxia reperfusion injury, promoting glucose consumption of cells, and protecting vascular endothelial cells from oxidative damage, and have important applications on preparation of drugs for preventing and curing diabetes and cardia-cerebrovascular diseases such as hypertension, atherosclerosis, cerebral angiospasm, coronarospasm, myocardial infarction, heart failure, and diabetic complications.
US20060014811 Medicament for treatment of cancer A medicament for the prevention and/or treatment of cancers and the like which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is {circle around (1)} a fused polycyclic heteroaryl group wherein the ring which binds directly to —CONH— group in the formula (I) is a benzene ring, {circle around (2)} unsubstituted thiazol-2-yl group, or {circle around (3)} unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —CONH-E wherein E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —CONH-E wherein E has the same meaning as that defined above.
US6979741 Acetyl-CoA carboxylase inhibitors Acetyl Coenzyme A Carboxylase inhibitors, pharmaceutical compositions containing such compounds and the use of such compounds to treat for example, Metabolic Syndrome including atherosclerosis, diabetes and obesity.
US8383158 Methods and compositions to treat myocardial conditions Methods, devices, kits and compositions to treat a myocardial infarction. In one embodiment, the method includes the prevention of remodeling of the infarct zone of the ventricle. In other embodiments, the method includes the introduction of structurally reinforcing agents. In other embodiments, agents are introduced into a ventricle to increase compliance of the ventricle. In an alternative embodiment, the prevention of remodeling includes the prevention of thinning of the ventricular infarct zone. In another embodiment, the prevention of remodeling and thinning of the infarct zone involves the cross-linking of collagen and prevention of collagen slipping. In other embodiments, the structurally reinforcing agent may be accompanied by other therapeutic agents. These agents may include, but are not, limited to pro-fibroblastic and angiogenic agents.
CN102603769A Sulfur-containing chromone compound and preparation method thereof and application in preparation of antitumor drugs The invention discloses a sulfur-containing chromone compound and a preparation method thereof and application in preparation of antitumor drugs. The structure of the sulfur-containing chromone compound is shown in a formula (I), wherein a compound 1 is R1=R2=R3=H; a compound 2 is R1=R3=H, R2=CH3; a compound 3 is R1=R3=Ac, R2=H; a compound 4 is R1=R2=R3=Ac; a compound 5 is R1=R2=Ac, R3=H; a compound 6 is R1=Ac, R2=R3=H; a compound 7 is R1=(R)-MTPA, R2=R3=H; and a compound 8 is R1=(S)-MTPA, R2=R3=H. The compound 1 and the compound 2 are obtained by preparing and separating from fungus Penicillium oxalicum CCTCC AF 93256 fermentation liquid. The compound 1 is subjected to acetylation reaction to obtain the compound 3 to the compound 6; the compound 1 is subjected to Mosher esterification reaction to obtain the compound 7 and the compound 8. The sulfur-containing chromone compound provided by the invention has the activity for inhibiting the growth of malignant melanoma cells, lung cancer cells, cervical cancer cells, breast cancer cells, laryngeal carcinoma cells, liver cancer cells and intestinal cancer cells, therefore, the sulfur-containing chromone compound has good application prospect on preparation of antitumor drugs. See formula (I).
US7858602 identifying a patient who is exhibiting signs of Alzheimer's disease;measuring and identifying carbonic anhydrase enzymes, than administering non-toxic amount of vitamin D3 to promotes the natural generation of the cell-specific carbonic anhydrase enzymes; aging resistance A method for the treatment and prophylaxis of conditions of aging due oxidative stress and as growth factors of stem cells. Such conditions due to oxidative stress are associated with a decreased presence of one or more cell-specific carbonic anhydrase enzymes in the tissue of a subject. Such conditions include but are not limited to alzheimer's disease, parkinson's disease, multiple sclerosis, autism, lou gehrig's disease, huntington's disease, diabetes mellitus, amyloid diseases, atherosclerosis, arthritis, osteoporosis, cystic fibrosis. The method comprises administering to the patient a pharmaceutically effective, non-toxic amount of one or more compounds that increases the presence of one or more Carbonic Anhydrase Isozymes whose levels have been reduced in the subject. Such compound maybe the Cell Specific Carbonic Anhydrase Enzymes, a compound that when absorbed reacts or dissociates to form cell specific carbonic enzymes or a compound that when administered promotes the natural generation of the cell specific carbonic anhydrase enzymes within the subject. This method also uses one or more cells specific carbonic anhydrase as growth factors of stem cells for replacing tissues due to injuries or diseases in humans. These methods includes the administering of these compounds over an extended period of time ranging from 6 months until the subject dies.
WO2009030153A1 The roles of mirnas in the diagnosis and treatment of systemic lupus erythematosus The present invention belongs to biotechnical field, which discloses the uses of a series of miRNAs in the preparation of reagents or kits for the detection of systemic lupus erythematosus (SLE). Reagents or kits for the detections of expression levels of these miRNAs and thus for diagnosis of SLE are also disclosed. It is the first time to reveal and demonstrate the close correlation between these miRNAs and SLE. These miRNAs are new drug targets of the prophylaxis and treatment of SLE, and the regulations of the expression levels of the same are novel measurements for the treatment of the disease.
US7230026 Selected fused pyrrolocarbazoles The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
CA2301057C A method of administering liposomal encapsulated taxane Liposomal-encapsulated taxane or an antineoplastic derivative thereof or a mixture thereof is provided which is used to effect a therapeutically enhanced method of treating cancer. The liposomal encapsulated paclitaxel allows for administration to a patient, particularly a human patient, in less than one hour without substantial toxicity.
WO2009059239A3 REDUCING Aβ42 LEVELS AND Aβ AGGREGATION This document relates to methods and materials for reducing Aβ42 levels, reducing Aβ aggregation, or reducing both Aβ42 levels and Aβ aggregation. For example, this document provides methods and materials related to the use of agents (e.g., 5β-cholanic acid) to reduce Aβ42 levels and to reduce Aβ aggregation in mammals.
WO2007144889A3 Treatment of neurofibromatosis Disclosed are methods of treating neurofibromatosis by administering to a human in need thereof effective amounts of FTS, or various analogs thereof , or a pharmaceutically acceptable salt thereof , optionally, in combination with colchicine. Also disclosed are pharmaceutical compositions comprising FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof ; colchicine; and a pharmaceutically acceptable carrier.
US20130108603 Collagen production compound A topical skin care lotion includes materials for supplementing the production of collagen I and III includes a base of lipophillic or lipophobic material and at least one amino acid. The amino acids are alanine and glycine. Other components of the lotion include iron, vitamin C, manganese, silica and cherry fruit extract. Together, these components assist the body with the production of collagen and promote healing of damaged skin. Antioxidants are also provided to protect the skin from oxidative stress by ultraviolet sunlight and environmental hazards.
EP2054408A2 Heterocyclic compounds suitable for the treatment of diseases related to elevated lipid level The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
US7288550 Administering 2-butyl-1-[5-(methylsulfonyl)pentyl]-1H-imidazo[4,5-c]quinolin-4-amine or salts to induce biosynthesis of cytokines such as IFN- alpha and/or TNF- alpha; treating viral diseases Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
EP2433948A1 Use of a new class of nucleotide sugar as antibiotic or cytostatic agent The present invention relates to the use of a compound of the formula (A), its use in medicine and for the prophylaxis and/or treatment of infectious diseases. Also disclosed are pharmaceutical formulations containing at least one of the inventive compounds. The compounds are especially useful for prophylaxis and/or treatment of bacterial infection. Further part of the invention is a method for producing the compounds of the formula (A).
US20120058197 Compositions comprising water with deuterium for the prevention or treatment of allergic diseases and a process for the preparation thereof The invention relates to pharmaceutical and food compositions for the prevention or treatment of allergic diseases and a process for the preparation thereof. The process of the invention comprises mixing water having 0.01-135 ppm deuterium content (preferably prepared by known electrolysis or distillation) with usual additives, and formulating this mixture by usual pharmaceutical or food industrial methods to pharmaceutical or food products, preferably by applying standard flavors, aromas and other additives used in the manufacturing of medicines, non-alcoholic drinks or beer.
US8420679 Aminothiazole derivatives and their use as CRF receptor ligands Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotrophin releasing factor (CRF) antagonists.
US20100080788 Alginate and alginate lyase compositions and methods of use The invention features alginate and alginate lyase compositions and methods that are useful for the treatment of various conditions and diseases. The invention also provides kits and instructions for use.
WO2007149381A2 Compositions comprising a ptp-ase inhibitor and use thereof in treating cancer The invention encmpasses therapeutic compositions containing a pentavalent antimonial composition. The pentavalent antimonial can be sodium stibogluconate and pentamidine and biological. equivalents of said compounds. The therapeutic composition of this embodiment contains an effective amount of pentavalent antimonial that can be used in treating diseases. The types of diseases that can be treated with the present invention include, but are not limited to, the following: diseases associated with PTPase activity, immune deficiency, cancer, infections (such as viral infections), hepatitis B, and hepatitis C. The therapeutic composition enhances cytokine activity. The therapeutic composition may include a cytokine, such as interferon α, interferon β, interferon y, or granulocyte/macrophage colony stimulating factor. The composition may also include a second agent for treating cancer.
EP1589972A1 Benzoquinolizine-2-carboxylic acid-containing compositions This invention relates to topical compositions of an antibacterial benzoquinolizine-2-carboxylic acid, incorporated either as the single therapeutic ingredient in hitherto undescribed pharmaceutical compositions, or as an ingredient in novel combination with at least one agent selected from a retinoid, an antifungal agent, another antibacterial compound and/or a steroid/non-steroid anti-inflammatory agent, to processes for preparation of the compositions, to use of the compositions in preparation of a medicament, and to a method of therapeutic or prophylactic use of such a composition for the treatment of dermal, ophthalmic, otic and nasal infections, with or without attendant inflammation.
WO2007134578A1 Novel indol-pyrrol derivatives for the treatment of proliferative and inflammatory diseases The invention relates to novel indol-pyrrol derivatives of formula I which are suitable for the production of pharmaceutical compositions for the prophylaxis and/or treatment of a proliferative or inflammatory disease.
CN102861126A Tablet for relieving sore-throat and moistening throat The invention discloses tablet for relieving sore-throat and moistening throat, which belongs to the field of a biological medicine. The constituents of the tablets are as follows: borneol, menthol crystal, licorice powder, sorbitol, magnesium stearate, flos lonicerae powder and xylitol. The tablet for relieving sore-throat and moistening throat provided by the invention is obtained by mixing, drying and shaping the raw materials. The tablet for relieving sore-throat and moistening throat has multiple effects of clearing throat and benefiting throat, clearing away heat and toxic materials and diminishing swelling and relieving pain, and the like, and simultaneously has the treatment effects on the symptoms, such as hoarseness and acute pharyngitis. According to the tablet, the main components are herbal plant extracts, which are free from side effects after the tablet is taken, so that the tablet can be extensively applied to all people.
CN101264065A Racecadotril dropping pill and preparation thereof The invention provides a racecadotril pill which is a composition used for curing acute diarrhea. The racecadotril pill takes g or Kg as the unit and adopts the weight ratio that racecadotril to polyethylene glycol (4000 to 10000) to polyoxyethylene (40) stearate is equal to 1: 1: 1 to 1: 3: 3. The invention also relates to a preparation method, which means that pro rata matching -> making melt liquid and/or emulsion and/or suspension by heating for standby -> adjusting the temperature control system of pill machine -> dropping pill and forming -> removing condensing agent and drying. The racecadotril pill has the advantages of high bioavailability, rapid releasing speed and rapid marked effect. The preparation method of racecadotril pill has the advantages of simple production technology, low production cost, non-pollution of production process and high yield.
WO2011113981A1 Water-soluble pharmaceutical composition comprising at least one therapeutically active substance having hydrophobic properties and at least one compound selected from among sialoglycosphingolipids, glycosphingolipids or a mixture of sialoglycosphingolipids and glycosphingolipids The invention relates to water-soluble pharmaceutical compositions comprising at least one therapeutically active substance and at least one compound selected from among sialoglycosphingolipids, glycosphingolipids or a mixture of sialoglycosphingolipids and glycosphingolipids, in which at least one of the therapeutically active substances is a drug with hydrophobic characteristics. In particular, the invention relates to injectable sterile compositions formed by nanomicelles of glycosphingolipids or modified glycosphingolipids, which can be non-covalently coated with albumin and which allow the delivery and controlled release of highly hydrophobic molecules.
EP2731676A1 Novel fxr (nr1h4) binding and activity modulating compounds The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds (1). Z is selected from (a), (b), (c) or (d).
WO2010048452A2 Polycyclic compounds and methods related thereto The invention relates to a novel compound of formula I or pharmaceutically acceptable salts thereof as well as pharmaceutical, nutraceutical, and botanical drug compositions and therapeutic methods related thereto. In certain embodiments, the compounds are used for the treatment of abnormal cell growth, hyperproliferative disorders, and inflammatory diseases in mammals. In other embodiments, the invention encompasses methods to isolate and synthesize the compounds.
US20110312906 Treatment or reduction of menopausal symptoms There is described a method for the treatment or prevention of menopausal symptoms or osteoporosis wherein there is administered to a subject in need of such treatment a therapeutically effective amount of the isotlavone formononetin, or a method for the treatment or prevention of menopausal symptoms wherein there is administered to a subject in need of such treatment a therapeutically effective amount of the isoflavone daidzein, the isotlavone being optionally administered with one or more pharmaceutically acceptable adjuvants, carriers and/or excipients. Therapeutic uses and compositions/foods are also described, comprising daidzein or formononetin optionally in association with one or more pharmaceutically acceptable adjuvants, carriers, food components and/or excipients.
US20120214876 Seizure and Migraine Treatments using the Bone Homeostasis Drug Cinacalcet A novel pathogenesis underlying certain types of seizures and migraines is disclosed and the validated set of premises presented enable the deductive conclusion to be made that drugs that reduce the amount of calcium ions (Ca++) released from bone reduce seizure and migraine risk. The premises validated as true in the specifications include: 1) Known seizure and migraine triggers increase osteoclast mediated release of Ca++ from bone. 2) Increased Ca++ released from bone increases seizure and migraine risk by a) depolarization of nerve membranes, b) enhanced calcium channel mediated neurotransmitter release and increases muscle contractility by c) enhanced neurotransmitter release at the neuromuscular junction and d) enhanced removal of the tropomyosin block between actin and myosin. 3) Conversely, reducing Ca++ released from bone reduces seizure and migraine risk. 4) Cinacalcet reduces Ca++ released from bone. Therefore, cinacalcet reduces seizure and migraine risk.
US8658179 Glycosylated specificity exchangers The present invention is directed to ligand/receptor and antigen/antibody specificity exchangers comprising a saccharide or glycoconjugate. Methods of making these specificity exchangers and methods of using said specificity exchangers to treat or prevent human disease are described herein.
CN101524363A Artificial saliva The invention relates to artificial saliva, which comprises a plurality of inorganic salt, HPMC, a preservative, a flavoring agent and other components. The artificial saliva has the following advantages that: (1) the artificial saliva can rapidly improve symptoms of a patient suffering from xerostomia, and can maintain the function in a longer period; (2) the artificial saliva has good stability; and (3) the artificial saliva has a good mouthfeel when in use.
CA2854186A1 Administration of a bis(thiohydrazide amide) compound for treating cancers Administration of a bis(thiohydrazide amide) compound is found to be surprisingly effective at treating subjects with cancer. Methods of treating a subject with cancer comprising continuously administering a bis(thiohydrazide amide) compound, or administering a bis(thiohydrazide amide) compound such that a constant concentration of the compound is achieved in the subject, are disclosed.
WO2014134705A1 Quinoline sulfonyl derivatives and uses thereof The present disclosure relates to quinoline sulfonyl compounds, compositions comprising these compounds and their use, in particular for the treatment of cancer. In particular, the present disclosure includes compounds of Formula (I), and compositions and uses thereof.
WO2008123891A1 PTERIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula (I) The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.
US20100159033 Benzisoxazole modulators of d2 receptor, and/or 5-ht2a receptor The present invention relates to new benzisoxazole modulators of D2 receptors and/or 5-HT2A receptors, pharmaceutical compositions thereof, and methods of use thereof.
WO2007013842A1 Use of 4-((tert-butylimino)methyl) benzene-1,3-disulfonate n-oxide against maemorrhagic changes in the brain The use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the treatment or prophylaxis of haemorrhagic changes in the brain is disclosed.
US20050142123 Comprising droplets of Coenzyme Q-10 dispersed in a matrix of a modified polysaccharide or a gelatin; supplement for human and animal nutrition Novel powder compositions comprising droplets of Coenzyme Q-10 dispersed in a matrix of a modified polysaccharide or a gelatin are obtained by emulsifying Coenzyme Q-10 in a solution of the matrix components.
WO2006056760A1 A combination of n-(3-metoxy-5-methylpyrazin-2-yl)-2-(4-`1,3,4-oxadiazol-2-yl!phenyl)pyridine-3-sulphonamide and an anti-mitotic agent for the treatment of cancer A combination, comprising N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide and an anti-mitotic cytotoxic agent.
WO2009143558A1 Injectable formulations The invention provides injectable solutions of an analgesic or antipyretic comprising water and a pyrrolidone, in particular highly concentrated injectable solutions of paracetamol.
US20110230450 Platelet-activating factor (paf) analogs and uses thereof Disclosed are novel methods and compositions for treating inflammatory diseases and disorders, utilizing structural analogs of platelet activating factor (PAF).
WO2006063515A1 Use of radix sanguisorbae and its extract for preparing medicament to increase rbc and hemoglobin RADIX SANGUISORBAE, its total saponin extract and ursane-type triterpenide saponin of formula (I) are useful for preparing medicament to increase the contents of RBC and hemoglobin. They may be produced into preparation such as oral preparation or injection, with pharmaceutically accepted carriers or adjunctive ingredients. The preparation can increase the contents of RBC and hemoglobin significantly and can treat or prevent all kinds of anaemia, especially for anaemia caused by malfunction or exhaustion of bone marrow.
WO2009013633A4 Amorphous coprecipitates of atorvastatin pharmaceutically acceptable salts The present invention relates to stable amorphous co-precipitates of atorvastatin pharmaceutically acceptable salts with pharmaceutically acceptable excipients, method for the preparation, pharmaceutical compositions, and method of treating thereof. Advantageously, the amorphous co-precipitates of atorvastatin pharmaceutically acceptable salts of the present invention have improved physiochemical characteristics that assist in the effective bioavailability
WO2009131815A1 1,5-diphenyl-pyrrolidin-2-one compounds as cb-1 ligands CB-1 receptor inverse agonist compounds of Formula (I) and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia.
US20080274184 Extracellular matrix (ECM) combined with therapeutic agents; promoting tissue wound healing; reducing side effects This invention is directed to graft materials comprising an extracellular matrix (ECM) and therapeutic agents. This invention is also directed to methods of using the graft materials for healing of damaged or diseased tissues on a patient's body.
CN101417987B DPP-IV inhibitor with sulfonamide formyl piperazine structure The invention belongs to the technical field of medicine, and in particular relates to a compound of DPP-IV inhibitor with a structure of sulfonamide formyl piperazine as shown in a general formula (I), and a pharmaceutically acceptable salt or an isomer thereof, wherein R<1>, Ar, and Ar<1> are as defined in the description. The invention also relates to a method for preparing the compounds, a medicine composition containing the compounds, as well as application of the compounds in the preparation of the medicine for treating and/or preventing diabetes, non-insulin-dependent diabetes, high blood sugar, and insulin resistance.
CN103664929A Dasatinib polycrystalline form medicament and preparation method thereof The invention provides a new dasatinib polycrystalline form medicament and a preparation method thereof. In a powder diffraction spectrum of a dasatinib polycrystalline form matter III provided by the invention, diffraction peaks exist at 2 theta of 6.2 plus or minus 0.2, 12.0 plus or minus 0.2, 15.3 plus or minus 0.2 and 18.4 plus or minus 0.2. The crystal form prepared by the preparation method provided by the invention has good chemical stability and high purity. The preparation method has the advantages of mild process conditions, simplicity in operation, stable and controllable quality and high yield, and is suitable for industrial production.
CA2264592C Bioconjugates and delivery of bioactive agents The present invention relates to bioconjugates and the delivery of bioactive agents which are preferably targeted for site-specific release in cells, tissues or organs. More particularly, this invention relates to bioconjugates which comprise of bioactive agent and an organocobalt complex. The bioactive agent is covalently bonded directly or indirectly to the cobalt atom of the oragnocobalt complex. The bioactive agent is released from the bioconjugate by the cleavage of the covalent bond between the bioactive agent and the cobalt atom in the oragnocobalt complex. The cleavage may occur as a result of normal displacment by cellular nucleophiles or enzymatic action, but is preferably caused to occur selectively at a predetermined release site by application of an external signal. The external signal may be light or photoexcitation, i.e. photolysis, or it may be ultrasound, i.e. sonolysis. Further, if the photolysis takes places in the presence of a magnetic field surrounding the release site, the release of the bioactive agent into surrounding healthy tissue is minimized.
US20130045940 Composition comprising as active ingredient l-carnitine in combination with a solar filter, for the prevention and/or treatment of pathologies of the eye due to ultraviolet radiation It is described a composition in the form of eye drops or ointment, comprising as active ingredients L-carnitine or a physiologically acceptable salt thereof; and 3-Hydroxykynurenine O-β-DL-glucoside, useful for preventing or treating pathologies of the eyes due to ultraviolet radiation.
EP1729785B1 Eye drops consisting of filtered clayey water for treating glaucoma The invention concerns eye drops consisting of filtered and purified clayey water. Said eye drops are used for treating glaucoma, to reduce intraocular pressure.
CN102151260A Andrographolide and berberine combination and application thereof The invention discloses a medicinal combination which consists of andrographolide and derivative of the andrographolide and salt capable of being used in pharmacy, and berberine and derivative of berberine and salt capable of being used in pharmacy, and pharmaceutical adjuvant. The effect of the combination is better than that when the andrographolide or the berberine is independently used. The andrographolide and berberine combination has good effects of antibiosis, anti-inflammation, anti-tumor and blood sugar reduction.
CN101077337A Vitamin injection used for promoting female animal estrus and Increasing breeding and preparation method thereof The present invention discloses one kind of vitamin injection as female animal aphrodisiac and its preparation process. The vitamin injection has main components including vitamin A, vitamin D and vitamin E, and supplementary materials, including antioxidant, bacteriostat and oil for injection. It is suitable for cow, mare, sow, ewe and other female animal in the duration period, and has the functions of promoting growth, raising reproductive capacity, regulating immunity, etc.
US20110034422 Dendrimers for sustained release of compounds Dendrimer-based compositions and methods are provided, that are useful for administering pharmaceutical compositions to target cells and tissues for treatment of ocular diseases including macular degeneration, diabetic retinopathy, and retinitis pigmentosa.
CN101327189B Method for preparing nano alcohol liposome material with mark and treatment double-function The invention relates to a preparation method of nanometer ethanol liposome material with marking and treating dual-function, belonging to the technical field of nanometer materials. The invention adopts CdTe and CdSe synthesized in water directly or CdSe/ZnS core-shell semiconductor quantum dots, and 5-FU and hydrophilic quantum dots are dissolved and scattered in phosphate buffer. Phospholipid is ultrasonically dissolved in absolute ethyl alcohol, the phosphate buffer containing the 5-FU and the quantum dots is slowly dropped into the absolute ethyl alcohol in a steam mode in a sealed container through a constant pressure funnel, then the stirring is carried out for mixing, stirring is continued after the dropping is finished, suspension with 5-FU and quantum dots scattered in ethanol liposome is obtained after cooling at room temperature, and the nanometer ethanol liposome is prepared respectively through polycarbonate membrane with a film extruder. The invention provides material for the treatment of scar and skin disease.
US20100197672 Pyrrole compounds as inhibitors of mycobacteria, synthesis thereof and intermediates thereto The present invention relates to a compound having the general formula (3): synthesis, intermediates and uses thereof.
CN101524343A Application of valproate and salt-induced redifferentiation combined with <131> iodine thereof in treating poor differentiation/dedifferentiation thyroid cancer The invention relates to the application of valproate and salt-induced redifferentiation combined with <131> iodine thereof in treating poor differentiation/dedifferentiation thyroid cancer, belonging to the pharmaceutical field, in particular to the pharmaceutical use of the valproate and salt thereof. Sulfonyl rhodamine B (SRB) dyeing analysis is adopted to detect influence of the valproate and the salt thereof on cell proliferation of follicular thyroid cancer cell strain FTC-133 and cell proliferation of papillary thyroid cancer cell strain K1; RT-PCR detects NIS mRNA expression in FTC-133 and K1 cells induced by the valproate and the salt thereof, and variation of iodine uptake of thyroid cancer cells after induced is analyzed; the result shows that the valproate and the salt thereof can obviously inhibit the proliferation of the thyroid cancer cells, and the inhibition rate is also increased along with increase of concentration; the NIS mRNA expression of FTC-133 and the NIS mRNA expression of K1 are both increased after being induced, and radioactive <131> iodine uptake of cancer cells is also increased; the poor differentiation/dedifferentiation thyroid cancer can select radioactive <131> iodine to carry out treatment because of the radioactive <131> iodine uptake increase of the cancer cells.
CN101904865A Hydrotalcite dispersible tablet and preparation method thereof The invention provides a hydrotalcite dispersible tablet which comprises 75.7-85.5wt% of hydrotalcite, 6.0-17.1wt% of pre-gelatinized starch, 2.4-4.8% of low-substitutive hydroxy propyl cellulose or crosslinking carboxymethylcellulose odium, 0.8-2.6wt% of polyvinylpyrrolidone or hydroxypropyl methylcellulose, 0.2-1.0wt% of saccharin sodium salt or steviosin, 0-0.3 wt% of menthol crystal, 0.6-1.0wt% of magnesium stearate and 0.8-1.7wt% of talcum powder or silicon dioxide. Compared with the common dispersible tablet, the hydrotalcite dispersible tablet has short disintegrating time, and the disintegrated grain water solution is in the state of suspending solution. Compared with the hydrotalcite chewable tablet and the common tablet, the hydrotalcite dispersible tablet is more convenient and flexible in taking, thereby not only being capable of taking by means of sucking and swallowing, but also being capable of taking by means of dispersing after adding water or juice and the like. Compared with the hydrotalcite blending and suspending agent and the grains agent, the hydrotalcite dispersible tablet is more convenient for storing and transporting. The dispersible tablet has good dispersible status, is convenient for taking, can be fast disintegrated after taking, achieves the aim of fast acting after being distributed onto the surface of the gastric mucosa, has the same preparation technology as the common non-coating tablet, does not need special equipment, and has lower preparation cost.
US20060035876 Combination therapy of an SODm and a corticosteroid for prevention and/or treatment of inflammatory bone or joint disease The present invention relates to pharmaceutical compositions and methods of using such compositions for the treatment of inflammatory diseases of the bone and joints. The compositions comprise a catalyst for the dismutation of superoxide, which is a non-proteinaceous mimetic of superoxide dismutase, in combination with a corticosteroid. The combination is substantially more effective than either the superoxide dismutase mimetic or the corticosteroid given alone at the same dose. Treatment with the combination beneficially alters the progression of the inflammatory bone and joint disease as measured histologically in diminished bone resorption and infiltration of inflammatory cells; as measured radiographically in diminished joint erosion, and diminished bone erosion and osteophyte formation; and as measured histomorphometrically in decreased bone resorption measurements of eroded surface and/or osteoclast surface relative to bone surface, and increased bone formation measurements of osteoblast surface relative to bone surface.
WO2009109364A1 Substituted sulfonamide derivatives The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
CN1973824A Anticancer composition containing both platinum compound and Sirolimus The anticancer composition containing both platinum compound and sirolimus is one kind of slow releasing injection or slow releasing implant. The slow releasing injection consists of slow released microsphere and special solvent containing suspending agent. The platinum compound is selected from cisplatin, carboplatin, lobaplatin, etc; the slow releasing supplementary material is selected from polylactic acid, lactic acid copolymer, polifeprosan, etc; and the suspending agent is selected from sodium carboxymethyl cellulose, iodine glycerin, etc. The slow releasing injection and the slow releasing implant are injected or set into solid tumor to diffuse and produce synergistic curative effect.
CN101897530A Medicinal composition, pillow inner filler and tea pillow The invention relates to a medicinal composition for treating a pillow inner material. The medicinal composition comprises the following medicinal components: lavender, silkworm excrement, cassia seed, ginkgo leaves, mint, chrysanthemum, gypsum rubrum, elecampane, gypsum, pinellia tuber, platycodon root, setose thistle, red-rooted salvia root, willow leaf swallowwort rhizome and clove. The invention also relates to pillow inner filler treated by the medicinal composition, and further relates to a tea pillow made by the pillow inner filler. The tea pillow has the functions of nursing sub-health, relieving various pains, resisting bacteria, eliminating inflammation, purifying air and preventing various diseases.
US20070190054 Prevention and treatment of complement-associated disorders The present invention concerns a recently discovered macrophage specific receptor, CRIg, and its use in the prevention and treatment of complement-associated disorders, including complement-associated eye conditions, such as age-related macular degeneration (AMD) and choroidal neovascularization (CNV).
CN101926778A Pamidronate disodium freeze-dried powder injection and preparation method thereof The invention relates to a pamidronate disodium freeze-dried powder injection and a preparation method thereof. The pamidronate disodium freeze-dried powder injection comprises the following components in parts by weight: 8-15 parts of pamidronate disodium and 60-150 parts of freeze-dried excipient, wherein the freeze-dried excipient is selected from one or a mixture of dextran 40, lactose, fructose or cane sugar; and a proper quantity of pH regulator is added to regulate the pH value to 6.5-7.0. The preparation method of the invention comprises the following steps: taking 60-150 parts of the freeze-dried excipient, adding water to dissolve the freeze-dried excipient, mixing with 8-15 parts of the pamidronate disodium, and dissolving the mixture; utilizing the pH regulator to regulate the pH valve; and carrying out split charging in bottles, freeze-drying and sealing.
WO2012146666A1 Pyrrolotriazinone derivatives as pi3k inhibitors New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
CN102503894A 5-substituted methylene imidazolidine-2, 4-diketone derivative as well as pharmaceutical composition and application thereof The invention discloses a compound with a structure of general formula I and salt acceptable in pharmacy, wherein the definitions of R1, R2 and R3 are the same the definitions in instruction. The invention also discloses pharmaceutical composition formed by compound serving as an active ingredient or salt acceptable in pharmacy, and one or more carriers, excipient or diluting agent acceptable in pharmacy, and the pharmaceutical composition plays an effect on curing diabetes on the aspect of medicine.
US20110126767 Methods and compositions for increasing the hatchability of hatchery eggs The invention relates to a method for hatching of hatchery eggs comprising: (a) treating the egg shell surface with a coating composition comprising a coating agent, to form a coating on the surface of the egg's shell; and (b) incubating the egg under conditions to cause hatching to occur; wherein the yield of hatching of said hatchery eggs is improved as compared to control eggs not treated as defined in (a). The invention additionally relates to a composition for treating of hatchery eggs prior to incubation, wherein said composition comprising a coating agent, and wherein said composition improves the hatching yield of said hatchery eggs.
US20130281415 NEW CYCLOHEXYLAMINE DERIVATIVES HAVING ß2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES The present disclosure relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
CN101574329A Zolpidem tartrate film agent The invention discloses a zolpidem tartrate film agent and a preparation method thereof. The film agent comprises the following components by weight percentage: 1-40 percent of zolpidem tartrate, 40-98 percent of high molecular film-forming material, 0-20 percent of plasticizer, 0-3 percent of titanium dioxide, and 1-30 percent of flavoring agent. The high molecular film-forming material comprises more than one of the following components of hydroxypropyl methylcellulose, hydroxy propyl cellulose, polyvinyl alcohol, polyvinyl pyrrolidone, sodium alginate, polyoxyethylene, bletilla mucilage, cornstarch, or carrageenan. The film agent has rapid dissolving out speed, good stability and rapid absorption, can release medicaments on the surface of a mucosa which then can absorb the medicaments quickly, and avoid the first-pass effect of liver, and has high bioavailability, is convenient in use, quick in effect, good in adaptability, popular by patients, has good formability, can be adhered at the drug administration position after drug administration, keeps the drugs not to be dispersed, can keep the original state to release the drugs continuously, is accurate in dosage, has no dust explosion during the production process, and can solve the problems of labor security and environmental pollution.
US7226939 Thienopyridine analogues with antifungal activity and process thereof The invention relates to novel antifungal compounds and its pharmaceutically acceptable salts, having as part of its structure, imidazolyl or benzimidazolyl derivatives. The imidazolyl derivative may be substituted at 2 position from among the group consisting of aroyl, p-chloroaroyl, phenyl hydroxy methine or p-chloro phenyl hydroxy methine or with n-butyl at 2 position and chlorine at 4 and 5 position. In the alternative, when it is a benzimadazolyl derivative, with hydrogen at 6 position, the substituent at 2 position may be selected from among methyl, ethyl, isopropyl, 2-oxopropl-1-yl, n-propyl, methoxy methyl, propen-1-yl, phenyl, p-chlorophenyl, p-toluyl, benzyl, 4-pyridyl, p-methoxy phenyl, 3-pyridyl, o-methoxy phenyl, styryl, 2-cyano methyl, p-hydroxy phenyl, p-amino phenyl, p-toluyl sulfonyl methyl or p-(t-butyl) phenyl group and if hydrogen is at 2 position, the substituent at the 6 position is selected from among nitro, trifluoromethyl or methoxy group.
CN101305995A Sustained release preparation containing domperidone pantoprazole sodium and its preparation method The invention relates to a compound preparation containing domperidone and pantoprazole sodium, and a preparation method. In the compound preparation, the domperidone comprises a sustained-release part and an immediate-release part, and the pantoprazole sodium is a common release component. The invention discloses a preparation method of the compound preparation.
US20100324123 Glms riboswitches, structure-based compound design with glms riboswitches, and methods and compositions for use of and with glms riboswitches The glmS riboswitch is a target for antibiotics and other small molecule therapies. Compounds can be used to stimulate, active, inhibit and/or inactivate the glmS riboswitch. The atomic structures of the glmS riboswitch can be used to design new compounds to stimulate, active, inhibit and/or inactivate riboswitches.
US7101887 Treating neuropsycological diseases; schizophrenia, psychotic depression and mania Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1–C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1–C4 alkyl, C1–C4 alkoxy, alkylthio, hydroxy, amino, mono(C1–C4)alkylamino, di(C1–C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.
US20100234311 Methicillin-Resistant Staphylococcus Aureus Active Metabolites This present provides kaempferol-3-(2-E,3-Z-di-p-coumaroyl)-rhamnoside, kaempferol-3-(2-Z-3-E-di-p-coumaroyl)-rhamnoside, and kaempferol-3-(2,3-di-Z-p-coumaroyl)-rhamnoside compounds useful as a new class of anti-bacterial agents. These compounds are extracted from Platanus occidentalis. These compounds were found to exhibit anti-bacterial activity against methicillin resistant Staphylococcus aureus (MRSA).
EP2667872A2 Small molecule rnase inhibitors and methods of use Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease.
US8273895 NK1 antagonists A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
WO2011084610A1 Liposomes for preventing the spread of hiv Formulations for preventing the sexual transmission of the HIV virus are provided. In one embodiment, the formulations contain unconjugated liposomes whose physicochemical properties allow binding to the HIV virus. The liposomes are made up of natural or synthetic lipids, alone or in combination. Preferably, the liposomes are made entirely of cardiolipin. In other embodiments the liposomes are modified to contain Hgands which bind HIV. The method for preventing the sexual transmission of the HIV virus includes self-administration of a formulation containing an effective amount of liposomes which bind to the HIV virus to the surface of a mucosal membrane prior to intercourse.
US8133894 N-benzyl-4-methyleneamino-3-hydroxy-2-pyridones Compounds of Formula (I) are effective in the treatment of a microbial infection.
WO2013123218A1 Selective estrogen receptor modulators with short half-lives and uses thereof The present invention relates to the long-term administration of a selective estrogen receptor modulator (SERM) with a short half-life for the treatment of a variety of estrogen receptor-mediated conditions. The SERM may be administered at a concentration at or below that of a SERM with a long half-life in order to achieve an equivalent therapeutic effect.
CA2151383C Stabilized medicinal aerosol solution formulation Stabilized medicinal aerosol solution formulations comprising medicaments that degrade or decompose by interaction with solvents or water, an HFC propellent, a cosolvent and an acid are described. Further, specific medicinal aerosol solution formulations comprising ipratropium bromide or fenoterol, ethyl alcohol, 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoropropane, and either an inorganic acid or an organic acid are described. The acids ace present in amounts sufficient to reduce the degradation of the medicaments to acceptable levels.
CN103520167A Long-acting injection comprising cefquinome sulfate and methanesulfonic acid danofloxacin The invention relates to preparation that acetic acid isobutyric acid sucrose ester is used in an oil-based injection for veterinary use, in particular to a compound long-acting injection which comprises methanesulfonic acid danofloxacin and cefquinome sulfate. The acetic acid isobutyric acid sucrose ester and hydrogenated castor oil are combined to be used for preparing the compound long-acting injection. A dispersion medium is one or the mixture of more than one of tetradecanoic acid isopropyl ester, benzyl benzoate and ethyl oleate. The injection is good in buffering effect, stable in character, good in histocompatibility and easy to prepare.
WO2009103754A3 Novel use of 3,3'-diindolylmethane The present invention relates to a novel use of 3,3'-diindolylmethane (CAS1968-05-4) and/or its derivatives in the form of a pharmaceutical and/or nutritional composition to retard or delay typical signs of aging and/or age-related pathological changes.
WO2013189847A1 Bendamustine derivatives and related compounds, and medical use thereof cancer therapy The present invention relates to bendamustine derivatives and related compounds of formula (VII), (VIII) and (IX), and medical uses thereof in particular in cancer therapy.
CN101669971A Compound extracted from shark cartilage marrows The invention provides a compound extracted from shark cartilage marrows. A main active component of the compound is 50 to 60 percent of chondroitin sulfate in percentage by weight. The molecular weight of the compound is between 21 and 100 Kilo Daltons, while heat contained in every 100 grams of the compound is between 300 and 350 Kilocalorie. The compound extracted from the shark cartilage marrows has the functions of preventing melanoma, neutralizing gastric acid, promoting blood circulation and the like.
WO2008003067A3 Methods and compositions for improved uptake of biological molecules A 'one-step' process for production of peptides and other organic molecules which are both esters and also acetylated forms of the desired molecule. The ester may be a mono-ester, di-ester, or another poly-ester, complexed with a molecule for protecting the organic molecules in the digestive tract. The method allows simple adjustment of the delivery properties of the peptides produced, in particular adjustment or addition of lipiphilic tendencies. A therapeutic or nutrient made by this method comprises acetylated organic molecule esters, in particular an acetylated peptide ester or even an acetylated amino acid ester and demonstrates improved metabolic properties leading to increased efficiency for therapeutic and cosmetic purposes including oral, transdermal, sublingual, buccal, and topical administration. The present disclosure further teaches several specific examples of acetylated esters, including acetyl-glutathione-ester (mGSH), MCAR (carnosine), pyruvate and others modified from base forms by the methods of the present disclosure.
EP1541576A1 Furoisoquinoline derivative and use thereof The present invention provides a compound represented by the formula wherein A represents (1) a bond, (2) a group represented by the formula -CRa=CRb- (Ra and Rb each represent a hydrogen atom or C1-6 alkyl) and the like; R1 represents (1) cyano or (2) an optionally esterified or amidated carboxyl group; R2 represents (1) a hydrogen atom, (2) an optionally substituted hydroxy group, (3) an optionally substituted amino group and the like; R3 and R4 each represent a hydrogen atom and the like; R5 represents a hydrogen atom and the like; R6 represents an optionally substituted hydroxy group and the like; R7and R8 each represent an optionally substituted hydrocarbon group and the like; R9 and R10 each represent (1) a hydrogen atom and the like; Y represents an optionally substituted methylene group; and n represents 0 or 1, or a salt thereof, which has an excellent phosphodiesterase IV inhibiting action.
US20100273819 3,3'-Spiroindolinone Derivatives There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, W, W′, V, V′, V″, R1, R2 and R3 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.
US7262187 Substituted oxazolo- and thizaolopyrimidinones as a mitotic kinesin inhibitor The present invention relates to azolopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
WO2008132443A1 Use of sapacitabine to treat proliferative disease One aspect of the present invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating a proliferative disorder, wherein the sapacitabine or metabolite thereof is administered in a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine or metabolite thereof for about 2 to about 6 days per week, for 2 weeks out of 3 weeks. Another aspect of the invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL).
EP1377269B1 Encapsulated dyes in cosmetic compositions The invention relates to a topical composition for application to skin comprising a cosmetically or pharmaceutically acceptable encapsulated liquid UV-absorbing naphthopyran or naphthoxazine dye, or a combination thereof, in combination with a cosmetically or pharmaceutically acceptable carrier.
US20090227501 Agents for preventing and/or treating upper digestive tract disorders A compound or its salts that inhibit the activity of the polypeptide or receptor of the present invention and the antibody of the present invention as well as the antisense DNA of the present invention are useful as, e.g., gastric acid secretion inhibitors, mucosa protectants, mineral absorption promoters, etc., which are less toxic and safe, and can be used as, e.g., agents for preventing/treating upper digestive tract disorders, antibacterial agents to Helicobacter pylori, etc. A compound or its salts that promote the activity of the polypeptide or receptor of the present invention, the polypeptide or receptor of the present invention and the DNA of the present invention can be used as, e.g., gastric acid secretion promoters and can be used as, e.g., agents for preventing/treating dyspepsia, bone metabolism disorders, anemia, etc. A compound or its salts that promote the activity of the polypeptide or receptor of the present invention, the polypeptide of the present invention, etc. can also be used as test agents for gastric secretory function. Furthermore, the polypeptide or receptor of the present invention and the DNA of the present invention are also useful for screening the agents for the prevention/treatment described above.
EP1638582B1 Use of hyaluronic acid for preparing compositions for treating recurrent oral cavity aphthas Use of hyaluronic acid as the sole active ingredient for preparing compositions in particular for topical use for treating oral cavity aphthas.
US20080166344 Coadministration of 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide and carboplatin; kits The present invention relates to a method of treating cancer by co-administration of an effective amount of 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide and an effective amount of one or more anticancer agents selected from the group consisting of carboplatin, cisplatin, paclitaxel, vinorelbine, gemcitabine, irinotecan, docetaxel, doxorubicin, dacarbazine and rituximab, or a retuximab-containing combination therapy selected from R-ICE and R-DHAP. The treatment method of the present invention is useful for the treatment for all solid tumors and lymphomas, preferably skin cancer, bladder cancer, breast cancer, uterine cancer, ovary cancer, prostate cancer, lung cancer, colon cancer, pancreas cancer, renal cancer, gastric cancer and the like. Particularly, they are expected as therapeutic agents for tumor types which show resistance against existing anticancer agents.
CN102512378A Stable and safe oxiracetam pharmaceutical composition for injection The invention relates to a stable and safe oxiracetam pharmaceutical composition for injection and a preparation method thereof, especially to an oxiracetam pharmaceutical composition for treating brain damage and neurological deficit caused by the brain damage as well as impediment of anamnesis and aptitude. Preferred are injections and lyophilized powders. The oxiracetam pharmaceutical composition provided by the invention mainly contains active components of oxiracetam, sodium chloride and citric acid. The oxiracetam pharmaceutical composition for injection has stable pH values and low impurity content. By the adoption of the preparation method, curative effects of the product are effectively raised, side effects are minimized, and simultaneously the yield is raised, cost is reduced, and higher benefits are created.
US20090221621 Methods of Reducing Alcohol-Induced Dose Dumping for Opioid Sustained Release Oral Dosage Forms Disclosed are methods of sustained release administration of opioids, including but not limited to hydromorphone and oxycodone, that exhibit improved properties with respect to co-ingestion with aqueous alcohol.
WO2009069014A1 Amorphous lamivudine and its preparation The present invention relates to amorphous lamivudine. The present invention further relates to a process for the preparation of amorphous lamivudine by spray drying.
CN101919818A Method for preparing tetrandrine lung-targeted controlled-release microspheres The invention belongs to the field of medicaments and hygiene and relates to a method for preparing tetrandrine lung-targeted controlled-release microspheres. The method comprises the following steps of: preparing tetrandrine serving as a medicament into solution; and preparing one of polylactic acid, chitosan and gelatin serving as a high-polymer auxiliary material into solution; mixing the solution according to a certain proportion; and performing ultrasonic emulsification, coagulation, solidification, centrifugal separation and drying under a specific condition to obtain the tetrandrine microspheres. The method can obtain lung-targeted controlled-release microspheres. The microspheres have the advantages of small particle size, high medicament carrying rate, medicament application effect superior to that of microspheres prepared by the conventional method, high chemical stability and microorganism stability, controllable method and process and stable quality.
CN103705460A Preparation method of enzymatic cross-linking medicine carrying nano micelle The invention relates to a preparation method of an enzymatic cross-linking medicine carrying nano micelle. The preparation method comprises the following steps: carrying out self-assembling to prepare a polymer micelle system by using a thermosensitive amphiphilic block copolymer, introducing a phenol group capable of generating cross-linking reaction into a thermosensitive block, catalyzing peroxidized hydroxide phenol group by Peroxidase to generate cross-linking reaction to obtain a nuclear crosslinking polymeric micelle, wherein the lowest critical micelle concentration is remarkably lower than that of nano micelle which is not cross-linked; when the micelle is prepared, adding adriamycin, taxol or camptotheca acuminate to prepare the enzymatic cross-linking medicine carrying nano micelle. The preparation method provided by the invention has the advantages that compared with conventional cross-linking methods, the preparation method has the advantages of safety, no toxicity, quick cross linking and the like, and is simple and convenient to operate, and has a good application prospect; the enzymatic cross-linking medicine carrying nano micelle has lower critical micelle concentration, so that the stability is improved, the circulating time of the micelle in blood can be prolonged and the efficiency that the micelle is endocytosed by tumor cells is increased, thereby further improving the bioavailability and the therapeutic effect of the medicine.
EP1268404B1 Malonamic acids and derivatives thereof as thyroid receptor ligands The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula (I), which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression and osteoporosis. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.
WO2007030361A3 Benzimidazole thiophene compounds as plk inhibitors The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents (formulaes A to H).
CN101678013A piperidine/piperazine derivatives The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C(=O)-; -C(=O)-C(=O)-; -NRX-C(=O)-; -Z-C(=O)-; -Z-NRX-C(=O)-; -C(=O)-Z-; -NRX-C(=O)-Z-; -C(=S)-; -NRX-C(=S)-; -Z-C(=S)-; -Z-NRX-C(=S)-; - C(=S)-Z-; -NRX-C(=S)-Z-;Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C(=O)-NRX- or -NRX-C(=O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3- dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl,C1-4alkyl substituted with hydroxyl; provided that the following compounds (A), (B) are excluded. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.
CA2155434C Prohormone convertase transformed cells and polypeptide synthesis Described is the production of mammalian cells expressing prohormone convertase which facilitates the processing of prohormone precursors to active hormones. Also described are variant prohormone convertases, and prohormones. The transformed cells of the present invention may be used in the synthesis of properly processed polypeptide hormones, and in cell culture to reduce dependence upon added hormones and required serum polypeptide factors.
EP1596874A1 Method for treating liver cancer by intrahepatic administration of nemorubicin The present invention relates to a treatment schedule of nemorubicin administered via the intrahepatic artery in a dosage ranging from about 100 mcg/m2 to about 800 mcg/m2 every 6 weeks to patients with a liver cancer.
CA2051693C Allosteric hemoglobin modifiers Allosteric hemoglobin modifier compounds having general structural formula (I) wherein X and Z may be CH2, NH or O.
US20080187492 Determining whether a compound, an inhibitor of a glutamate receptor, reduces Fragile X syndrome, a tauopathy, Huntington's disease, neurofibromatosis 1, Parkinson's disease of an analogous disease in a Drosophila Methods of evaluating a compound for the ability to reduce a mental defect in a metazoan are provided, where the mental defect is caused by Fragile X syndrome, a tauopathy, Huntington's disease, neurofibromatosis 1, Parkinson's disease. The methods comprise determining whether the compound reduces a mental effect of the analogous disease in a Drosophila melanogaster Also provided are methods of evaluating a compound for the ability to improve learning or memory in a mammal. The methods comprise determining whether the compound improves learning or memory in a Drosophila melanogaster that is deficient in a dFRM1. Additionally, methods of treatment of a mammal deficient in expression of an FMR1 gene are provided. The methods comprise treating the mammal with a compound in a pharmaceutically acceptable excipient, where the compound inhibits expression or activity of a group II or group I metabotropic glutamate receptor (mGluR), an inositol trisphosphate receptor (InsP3R), a glycogen synthase kinase-3β (GSK-3β), or a phosphodiesterase-4 (PDE-4) in the mammal.
WO2013147000A1 Aqueous composition containing 2-amino-3-(4-bromobenzoyl)- phenylacetic acid The present invention pertains to an aqueous composition which contains 2-amino-3-(4-bromobenzoyl)phenylacetic acid or a salt thereof and which may contain, if necessary, a benzalkonium chloride and/or a polyoxyethylene sorbitan fatty acid ester. The stability of 2-amino-3-(4-bromobenzoyl)phenylacetic acid or a salt thereof can be kept by restricting the contents of a benzalkonium chloride and a polyoxyethylene sorbitan fatty acid ester respectively within specific ranges, whereby a composition which does not suffer any appearance change can be obtained.
CN103739456A New derivative of 2-(p-((Z-4-chloro-1,2-diphenyl-1-butenyl) phenoxy) ethanol and application thereof The invention discloses a new derivative of 2-(p-((Z-4-chloro-1,2-diphenyl-1-butenyl) phenoxy) ethanol and application thereof, the derivative has good drug activity, can greatly increase the half-life of a drug, prolongs the retention time of the drug in the human body, at the same time, improves the drug concentrations in the blood so as to achieve a better therapeutic effect. Because the half-life of the drug is greatly increased, the drug can be longer to maintain an activity concentration in the blood, so that in dose limiting treatment conditions, the therapeutic effect can be maintained meanwhile the use amount of the drug can be reduced, the adverse metabolic problems of the drug can be eliminated, the drug toxicity is reduced, and toxic and side effects in a drug use course can be reduced.
CN1723962A Application of total flavone of An application of Laoying tea total flavone in preparing the medicines for treating hyperlipemia type fatty liver is disclosed. Its advantage is high curative effect.
WO2012110840A1 Diaryl ether linked pyrrolo [2,1-c][1,4] benzodiazepine hybrids and process for the preparation thereof The present invention provides a compound of general formula A, useful as potential anticancer agents against eleven human cancer cell lines. The present invention further provides a process for the preparation of diaryl ether linked pyrrolo[2,1-c][1, 4]benzodi azepine conjugates attached through different alkane spacers of general Formula (A). General Formula (A) wherein R = Formula (I) or Formula (II) wherein R1, R2, R3 = H or OMe; X = NO2, NH2, F, I; n = 2, 3, 4 and 5.
CN1919321A Decoction medicine for treating stomatocace of asthenic fire flaring up type and its preparation method Disclosed is a medicinal broth for treating ulcerative stomatitis and its preparation, wherein the medicament is prepared from the following raw materials (by weight portion): astragalus root, plaster stone, codonopsis pilosula each 18-20g, dried orange peel 12-15g, scrophularia root, Chinese angelica root, poria cocos, corktree bark, alisol each 9-12g, bamboo leaves, and licorice root each 5-7g. The invention realizes easy material availability, simplified preparation, low cost, and quick effect.
WO2008128049A3 Tetrahydrobiopterin compositions and methods of measuring The present invention is directed to treatment methods of administering tetrahydrobiopterin, including in oral dosage forms, in intravenous formulations, and with food. Also disclosed herein are biopterin assays for measuring the amount of biopterin and metabolites of biopterin in a sample.
US20120289482 Method for modulating or controlling connexin 43(Cx43) level of a cell and reducing arrhythmic risk A method of modulating or controlling connexin 43 (Cx43) level of a cell includes inducing mitochondrial reactive oxygen species (ROS) production in the cell.
WO2012035794A1 Octreotide-modified nano preparation for treatment of cancer or palliative care of cancer The present invention relates to a pharmaceutical composition for the treatment, palliative care or prevention of cancer such as medullary thyroid carcinoma. Specifically, the present invention relates to a pharmaceutical composition for the treatment, palliative care or prevention of cancer such as medullary thyroid carcinoma, which contains a liposome modified with octreotide.
CN101804060B Microsphere injection of ceftriaxone sodium/tazobactam sodium drug composition The invention discloses microsphere injection of a ceftriaxone sodium/tazobactam sodium drug composition, which comprises ceftriaxone sodium, tazobactam sodium, PLA, sodium glycocholate, PEG600 and trehalose. In the preferential technical scheme, the microsphere injection comprises 3 parts of ceftriaxone sodium, 1 part of tazobactam sodium, 2.5-7 parts of PLA, 3-6 parts of sodium glycocholate, 2-5 parts of PEG600 and 8-15 parts of trehalose. Compared with the prior art, the invention has the advantages of good stability, high encapsulation efficiency, preparation process suitable for industrial production and proper slow-release effect.
CN101732266A Sibutramine hydrochloride chewable tablet and preparation method thereof The invention discloses a sibutramine hydrochloride chewable tablet, which is prepared from the following materials in percentage by weight: 0.1-15% of sibutramine hydrochloride, 15%-99.9% of a filler, 1%-15% of a disintegrant, 0.1%-5% of lubricant, 0.1%-5% of flow aid, 0.05%-5% of correctant, 0.01%-3% of sweetener and 0.01%-5% of odor-masking agent. The preparation method comprises the following steps of: taking the sibutramine hydrochloride, the correctant and the sweetener to mix according to the proportion, and then adding the odor-masking agent to granulate, drying and straightening granules; mixing the filler, the disintegrant and other assistant materials, and directly tabletting. The invention has advantages of convenient taking, good mouth feel, each absorption and rapid effect.
EP2127681A1 Therapeutic agent for periodontal disease and alveolar bone loss due to surgery By suppressing transcription activation by NFκB, the present invention was demonstrated to suppress alveolar bone resorption in periodontal disease models, and promote restoration of alveolar bone in periodontal disease-caused bone defect models. Therefore, the present invention provides agents for treating, preventing, and improving periodontal diseases and alveolar bone defects caused by surgical operations, said agents comprising as an active ingredient, a NFκB decoy or such that suppresses the transcription activity of NFκB.
US20100331315 Rhodanines and related heterocycles as kinase inhibitors The invention provides compounds that inhibit PIM kinases and/or CK2, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.
US7799356 Prophylaxis or treatment of inflammatory skin conditions A cosmetic or pharmaceutical preparation comprising licochalcone A and one or more hydrocolloids. This Abstract is not intended to define the invention disclosed in the specification, nor intended to limit the scope of the invention in any way.
EP1539147A4 Methods of treating microbial infections in humans and animals A method of treating a subject with a microbially-based infection, comprising the administration of a compound to the subject. The compound is able to decrease ATP levels in the microbe by at least 10% compared to controls after 24 hours in an in vitro test, without killing mammalian cells during the same time period. The decrease in ATP levels is measured by: (1) removing the cells from the testing location and putting them on ice; (2) harvesting the cells at 4 degrees C by centrifugation and disrupting it with bead-beating in an ATP extraction buffer; (3) removing cellular debris by centrifugation at 4 degrees C, leaving an ATP-containing supernatant; (4) measuring the amount of ATP present in the supernatant by a bioluminescence assay at 4 degrees C.
CN101842097A Biofilm treatment The invention provides a method of preventing, inhibiting or reducing a P. gingivalis biofilm in a subject comprising administering to the subject a pharmaceutical composition comprising an inhibiting agent of a polypeptide that reduces or inhibits biofilm formation and/or biofilm development. Also provided are compositions useful in the prevention, inhibition or treatment of periodontal disease or P. gingivalis infection.
US20060084613 Dipeptide enzyme inhibitor; antiinflammatory agents; autoimmune disease; wound healing agents This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds having the following structure: wherein A, B, R, R1, R1′ p and q are as defined herein. The invention is also directed to pharmaceutical compositions containing one or more of these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
WO2013153129A1 Combination of somatostatin-analogs with 11beta-hydroxylase inhibitors The present invention relates to a combination which comprises (a) a somatostatin analogue and (b) a 11beta-hydroxylase inhibitor; each in free form or in the form of a pharmaceutical acceptable salt thereof; the use of such a combination for the preparation of a medicament for the treatment of diseases associated with increased stress hormone levels; a commercial package or product comprising such a combination; and to a method of treatment of a warm-blooded animal, especially a human.
CN103690490A System and method for generating nitric oxide based on microencapsulated chemical reactants Methods and compositions are disclosed for generating extended release therapeutic nitric oxide including providing a mixture of two or more types of sub-millimeter-scale microparticles, where each type of particle contains only one kind of microencapsulated reactant. The mixture comprises at least one microencapsulated nitrite salt particle, at least one microencapsulated acid particle, and the microencapsulated reducing agent particles are slowly released through providing an activating volume of water sufficient to incipiently wet the submillimeter-scaled particles, wherein enough amount is represented for action for generating nitric oxide. The microencapsulated chemical reactants can be applied in hydrogel, and can be applied on a treatment part directly or through a medical apparatus (such as wound dressing or bandage). In the other applications, the microencapsulated chemical precursors are maintained in close physical proximity to one another in a limited volume, and a limited amount of solvent residing within that same volume is used to extract and process the reagents to form NO.
WO2007065664A2 Pyrazolo[1,5-a]pyridine-3-carboxylic acids as ephb and vegfr2 kinase inhibitors The invention relates to novel pyrazolo[1,5-a]pyridine-3-carboxylic acid compounds of the Formula (I) in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
CN102727425A Nitroimidazole oculentum and preparation method thereof The invention provides a nitroimidazole oculentum and a preparation method thereof, relating to a medicinal preparation for eyes. The nitroimidazole oculentum comprises an active component, an oculentum matrix and auxiliary materials, wherein the active component is metronidazole or tinidazole and the auxiliary materials comprise at least one of carrier, emulsifier, common medicinal fungistat for eyes; in percentage by mass, the contents of the active component, the oculentum matrix and the auxiliary materials are 0.5-3%, 95%-99% and 0-5%, respectively. The preparation method of the nitroimidazole oculentum comprises the following steps: heating and melting anhydrous lanolin and albolene, filtering and drying for sterilization; drying liquid paraffin for sterilization; putting metronidazole or tinidazole in a mortar, adding a part of the dried and sterilized iquid paraffin into the mortar, and grinding into fine paste; adding a part of the sterilized oculentum matrix to the paste and uniformly grinding; then adding the rest oculentum matrix and/or other auxiliary materials gradually while grinding, so as to reach the total amount; and finally carrying out sterile subpackage to obtain the nitroimidazole oculentum. The nitroimidazole oculentum can be used for treating mite blepharitis ciliaris and eye surface pathological changes.
WO2014146218A1 Usage of mycophenolate mofetil or salt thereof in preparing drug for resisting against influenza virus Disclosed is a usage of mycophenolate mofetil or pharmacologically acceptable salt thereof in preparing a drug for resisting against an influenza virus. Further disclosed is a usage of mycophenolate mofetil or pharmacologically acceptable salt thereof in preparing a drug for resisting against a drug-resistant phenotype influenza virus. The present invention also relates to a method for treating an influenza disease, comprising giving mycophenolate mofetil or pharmacologically acceptable salt thereof with an effective dose to an individual in need.
CN101352452A Pharmaceutical composition capable of preventing and treating oviduct adhesions The invention belongs to the technical field of medical treatment or medicines and relates to a novel medicine combination which can be used for preventing and treating pains and the possible situations such as infection, adhesion, and the like after uterine cavity operation. The main ingredients are sodium hyaluronate (also called sodium hyaluronate), antibiotics and local anaesthetics. The novel medicine combination is characterized in that: sodium hyaluronate is adopted to shield the pain conduction function of a pain receptor and can play the roles of physical brackets, moisture retention and moistening so as to prevent inflammation on a damage surface from spreading and to avoid tissue adhesion of the uterine cavity as well as the adhesion formed when tissue fragments flow back to the uterine tube; furthermore, sodium hyaluronate can prolong the local action time of antibiotics and local anaesthetics in the uterine cavity. By combining the functions of pain prevention, anti-inflammation and adhesion resistance into a whole, the medicine combination with the three ingredients can effectively prevent and treat pains, infection, adhesion, and the like problems after uterine cavity operation. Moreover, some functions of sodium hyaluronate are utilized for confining the local effects of the medicines, thus reducing the possibility of causing general adverse effects of the medicines.
WO2014024993A1 Piperazine derivative and use thereof Provided is a compound having an antagonistic activity on an arginine-vasopressin 1b receptor. A compound represented by general formula (I) [wherein each symbol is as defied in the description] or a salt thereof has an antagonistic activity on an arginine-vasopressin 1b receptor.
EP2050442A1 Pharmaceutical composition for prevention and/or treatment of bone disease, functional food or health food comprising the composition, and pharmaceutical preparation comprising the composition as active ingredient The present invention provides a highly safe pharmaceutical composition for preventing and/or treating bone disease, a pharmaceutical preparation comprising thereof, a health food comprising thereof, a functional food comprising thereof. Since the present invention comprises the arylheptanoid compound shown in the following formula (I) and the derivatives thereof, it enables to prevent and/or treat the bone disease. (In the formula (I), R1 and R5 are a functional group selected from the group consisting of a hydrogen atom, alkyl group having carbon numbers 1 to 3, monosaccharide and disaccharide; R2, R3, and R4 are a functional group selected from the group consisting of a hydrogen atom, an oxygen atom, alkyl group having carbon numbers 1 to 3, monosaccharide and disaccharide; R5 may be bound on meta-position against heptylene group of another aryl group to form a ring.)
CN103012295A Optical isomerism of andiconazole as well as preparation method and application of optical isomerism The invention belongs to the technical field of medicines, and specifically relates to an optical isomerism of a triadimenol antifungal candidate medicine. The invention provides the optical isomerism of a triazole alcohol compound with the chemical structural formula shown in the specification and salts of the optical isomerism. In the optical isomerism, C3 hydroxyl is in R configuration or S configuration. The invention also provides a preparation method of the optical isomerism of the andiconazole and an application of the optical isomerism in the preparation of the antifungal medicines.
US20090306088 Substituted heteroaryl pyridopyrimidone derivatives A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof are disclosed and claimed. Wherein m, n, o, Y, Z, R1, R2, R3, R4, R5 R6 and R7 are as described herein. Also disclosed are the salts of compounds of formula (I). The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.
EP2191718A1 Compounds and uses for the treatment of airway diseases and for the delivery of airway drugs Chronic obstructive airway diseases are treated by administering an osmotically active compound such as a salt, sugar, sugar alcohol, or organic osmolyte to the afflicted airway surface. The compound may be administered as a liquid or dry powder aerosol formulation. Diseases that can be treated by the method include cystic fibrosis, chronic bronchitis, and ciliary dyskinesia. The formulations of the invention can also be used in conjunction with other active agents such as bronchodilators, sodium channel blockers, antibiotics, enzymes, or purinoceptor agonists on airway surfaces.
CN101449659B Environment regulating agent and production method thereof The present invention relates to environmental regulator and a method of producing the same, comprising lysozyme, thrombin, modified montmorillonite power, fucose, eucalyptus oil, phytoncide and the like. Due to effects of drying, sterilization, hemostasia and adsorption and the like, the diseases of diarrhea, bacterial infection the like caused by coldness and dampness on pups are effectively improved, meanwhile hemorrhage of pups is restrained, thereby improving generating environment to ensure body conditions of the pups due to the regulator.
WO2005113537A3 Urea antagonists of p2y1 receptor useful in the treatment of thrombotic conditions The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
DE102010033301A1 Topically applicable medicament, useful for treating actinic keratosis, comprises diclofenac and chitosan Topically applicable medicament comprises diclofenac and chitosan. - ACTIVITY : Keratolytic; Dermatological. Test details are described but no results given. - MECHANISM OF ACTION : None given.
US20080153799 Novel Quinoline-Carbaxamides as Jak3 Kinase Modulators The present invention relates to novel compounds which are JAK3 Kinase inhibitors, methods for their preparation and pharmaceutical compositions comprising them. A compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein X is —CHOH or —C═O;
CN103239561A Domesticated sika deer fetus extract and preparation method thereof The invention discloses a domesticated sika deer fetus extract and a preparation method thereof and belongs to the technical field of medicines. The preparation method comprises the following steps of: drying 55-65 parts by mass of fresh domesticated sika deer fetus, 8-12 parts by mass of brown sugar, 8-12 parts by mass of jujube and 8-12 parts by mass of medlar at the temperature of 60-70 DEG C until the weight is constant, grinding respectively, passing a 80-mesh sieve, uniformly mixing, adding 3-5 parts by mass of soy isoflavone or female silkworm moth, 4-6 parts by mass of honey, 7-8 parts by mass of coagulator-agar powder and 120-130 parts by mass of de-ionized water, and uniformly mixing; sterilizing a mixed solution for 30 minutes under 0.1 MPa at the temperature of 121 DEG C; and slightly cooling, pouring the mixed solution into a round flat die, cooling until forming, taking out a sample, and drying for 3-4 hours at the temperature of 55-65 DEG C to obtain the domesticated sika deer fetus extract. The production process is simple and effective, the domesticated sika deer fetus extract can be conveniently stored and packaged and is convenient for a human body to take, and the development of the domesticated sika deer industry can be greatly promoted.
WO2014085914A1 Topical liposome compositions containing phenolic anti-inflammatory agents and their methods of preparation Liposomal topical compositions containing phenolic anti-inflammatory agents, and methods for making thereof, are presented. These compositions are generally used for helping to prevent solar radiation-induced skin damage and helping to prevent and/or treat inflammatory dry skin conditions caused by eczema and contact dermatitis.
US20100292222 Chemical compounds 751 The invention concerns bicyclic compounds of Formula (I) wherein, R1, R2, R3, R4, R5, X1, X2, Y, k, m, n and p are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.
US20100092578 Protein kinase c iota The invention involves PKCι signaling. The invention provides, for example, transgenic animals, inhibitors of PKCι signaling, methods for inhibiting PKCι signaling, methods for identifying inhibitors of PKCι signaling, and methods for diagnosing cancer.
CN1857439A Preparation and application of ginkgo leaf flavonid composition The present invention relates to compound preparation with gingko leaf flavonid composition as main component for treating cardiac and cerebral vascular diseases. The gingko leaf flavonid composition contains gingko leaf flavonid in 1-99 wt%, and sowthistle-leaf ixeris flavonid and saponin, pueraria flavonid, safflower flavonid, total astragalus flavone and saponin, general peony glycosideor seabuckthorn flavonid in 1-99 wt%, and is compounded with pharmaceutically acceptable supplementary material to prepare pharmaceutically acceptable preparations. The medicine of the present invention is used in preventing and treating cardiac and cerebral vascular diseases, senile dementia, and other diseases.
CN102871978A Levosulpiride tablets and preparation method thereof The invention provides levosulpiride tablets and a preparation method thereof. The levosulpiride tablets comprise levosulpiride, microcrystalline cellulose, crosslinking povidone and magnesium stearate, and have the advantages of simple prescription, high production efficiency, energy saving and cost saving; and the prepared tablets have the characteristics of quick disintegration and dissolution as well as good stability.
WO2009061906A3 Treating protein misfolding diseases This document provides methods and materials related to treating a protein misfolding disease. For example, methods and materials relating to the use of a lobeline compound to treat a protein misfolding disease are provided.
US20120004166 Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament The invention relates to aryloxyalkylene-substituted hydroxyphenylhexynoic acid derivatives, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 and A are each defined as specified, and physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
CN101262906A JNK inhibitors for the treatment of endometreosis This invention relates to a method of treating and/or preventing endometriosis comprising administering a JNK inhibitor. The JNK inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis-related infertility.
CN103099780A Preparation method of hydrogen-microbubble-containing aqueous solution, and product and application of method The invention relates to a novel hydrogen-containing medicine dosage form. Hydrogen is made into a hydrogen-microbubble-containing aqueous solution in a manner of coating by phospholipid, so that the hydrogen content of the solution can greatly increase, the hydrogen concentration can be controlled, and the hydrogen is more stable. In addition, by virtue of a microbubble technology, the hydrogen-microbubble-containing aqueous solution can also be taken as an ultrasonic contrast agent and has multiple function effects.
WO2004093916A8 A medicament for the two-step perioperative therapy of solid tumours The present invention describes the use of an agent endowed with tumour tropism in combination with another agent with anticancer activity and with an affinity for the first agent for the preparation of a medicament useful for the two-step perioperative therapy of solid tumours. The advantages of the present invention consist in the greater, effective localisation of its anticancer activity, in the reduction of the number of administration steps and in the possibility of reducing the anticancer doses, with a resulting decrease in side effects, but without any loss of efficacy.
WO2005051286A2 Stable ready-for-use injectable solution of 9-((1,3-dihydroxypropan-2-yloxy) methyl)-2-amine-1h-purin-6(9h)-one. The present invention describes a sterile, stable and ready-for-use injectable solution comprising 9-((1,3-dihydroxypropan-2-iloxy)methyl)-2-amino-1H-purin-6(9H)-one in glucose 5% aqueous solution or sodium chloride 0.9% aqueous solution. It also describes a closed system used for packing the solution, which consists of a flexible bag manufactured with a tri-laminated material. The present invention also describes a process for eliminating the residual alkalinity that is present in the 9-((1,3-dihydroxypropan-2-iloxy)methyl)-2-amino-1H-purin-6(9H)-one, so obtaining crystals that are free from alkaline residues and suitable for the direct preparation of the solution. The present invention relates to the medical and therapeutic areas, mainly for treating immunodepressed patients carrying viral infections.
CN103610662A Glycyrrhizin capsule The invention discloses a glycyrrhizin capsule, which consists of the following raw materials in parts by weight: 700-800 parts of mono potassium glycyrrhizinate tablets, 290-310 parts of calcium carbonate, 600-700 parts of microcrystalline cellulose, 45-55 parts of sodium carboxymethyl starch and a proper amount of 75 percent ethanol. According to the glycyrrhizin capsule, novel auxiliary materials, having high bond resistance and disintegrating functions, such as the calcium carbonate, the microcrystalline cellulose and the sodium carboxymethyl starch are adopted, so that the prepared capsule can be disintegrated and dissolved out rapidly, medicines can be dissolved by almost 100 percent within 10 minutes, the absorption and utilization of the medicines are ensured effectively, the bioavailability of the medicines is increased, a good treatment effect is achieved, a good news is brought to patients suffering from hepatitis, and a good social benefit is achieved.
US7517658 Drug screening for human SNORF33 receptor agonist by contacting cells transfected with and expressing DNA encoding the human SNORF33 receptor, wherein cells prior to being transfected with the DNA do not express the human SNORF33 receptor; inflammation, infections, arthritis; autoimmune diseases This invention provides isolated nucleic acids encoding mammalian SNORF33 receptors, purified mammalian SNORF33 receptors, vectors comprising nucleic acid encoding mammalian SNORF33 receptors, cells comprising such vectors, antibodies directed to mammalian SNORF33 receptors, nucleic acid probes useful for detecting nucleic acid encoding mammalian SNORF33 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding mammalian SNORF33 receptors, transgenic, nonhuman animals which express DNA encoding normal or mutant mammalian SNORF33 receptors, methods of isolating mammalian SNORF33 receptors, methods of treating an abnormality that is linked to the activity of the mammalian SNORF33 receptors, as well as methods of determining binding of compounds to mammalian SNORF33 receptors, methods of identifying agonists and antagonists of SNORF33 receptors, and agonists and antagonists so identified.
CN103610874A Drinking water for treating sore tongues The invention relates to drinking water for treating sore tongues. The drinking water consists of the following components in parts by weight: 40-50 parts of impatiens balsamina, 40-50 parts of artemisia anomala, 40-50 parts of native copper, 20-30 parts of radices trichosanthis, 20-30 parts of fel ursi, 20-30 parts of Chinese thorowax root, 20-30 parts of chrysanthemum and 5-15 parts of rhizoma dioscoreae bulbiferae. In the drinking water provided by the invention, impatiens balsamina has the functions of invigorating the circulation of blood to relieve swelling and pain, the artemisia anomala can break blood to stimulate the menstrual flow and relieve pain, the native copper can be used for removing stasis to relieve pain, and the three components are monarch medicines of one another; the radices trichosanthis can be used for removing heat, promoting salivation, removing swelling and eliminating pus, the fel ursi can be used for clearing the heat and toxic materials, the Chinese thorowax root can be used for soothing liver-qi stagnation, the chrysanthemum can be used for clearing away heat and toxic materials and removing wind-heat, and the components are ministerial medicines of one another; rhizoma dioscoreae bulbiferae can be used for removing stasis, removing goiter, cooling the blood and stopping bleeding, and is used as an adjuvant medicine. The drinking water is reasonable in component and capable of effectively treating sore tongues.
EP2637665A1 Dexamethasone combination therapy The present invention relates to a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I), as described herein, and/or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, and an amount of (2) dexamethasone and/or a pharmaceutically acceptable salt, solvate, metabolite or racemate thereof, such that the subject is treated. In another aspect, provided herein is a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I) and an amount of (2) dexamethasone, such that the subject is treated; pharmaceutical formulations comprising said combination for the treatment of multiple myelom; and compositions thereof.
CN103508930A Bis(aminodithioformate)-1,3-propane diester compound, and synthesis method, pharmaceutical composition and use thereof The invention relates to a bis(aminodithioformate)-1,3-propane diester compound, and synthesis method thereof, a pharmaceutical composition containing the compound and a use, and especially relates to the use in preparing drugs for treating or preventing cancers. The compound is represented as the formula (I), wherein A is selected from substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic group, R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl alkyl or heteroaryl alkyl, or a substituted or unsubstituted heterocyclic ring formed together by the R1, the R2 and an N atom connected with the R1 and the R2.
EP1945267A2 Small interfering oligonucleotides comprising arabinose modified nucleotides Small interfering ribonucleic acid duplexes (siRNA) comprising at least one arabinose modified nucleotide that inhibit gene expression are Provided. In one embodiment, the duplexes contain ribonucleotides wherein at least one arabinose modified nucleotide is a 2'-deoxy-2'- fluoroarabinonucleotide (FANA).
EP1651198A2 Selective pharmacologic inhibition of protein trafficking and related methods of treating human diseases Preferred aspects of the present invention relate to the inhibition of intracellular protein trafficking pathways through selective pharmacologic down-regulation of specific resident ER and golgi proteins, and more particularly, to methods of treating a variety of disease conditions, which depend on these intracellular protein trafficking pathways.
EP1861113B1 Use of an onion extract for making a composition to control weight gain The invention concerns the use of an onion extract comprising 20 wt. % to 40 wt. % of polyphenols of the flavonol family, said onion extract having the following composition characteristics, expressed in weight relative to the total extract dry weight: 60 wt. % to 90 wt. % of the total flavonols of said extract consist of glycosylated polyphenols; 85 wt. % to 98 wt. % of total flavonols of said extract consist of free-form (aglycon) or glycosylated quercetin; 5 wt. % to 20 wt. % of the total flavonols of said extract consist of quercetin-3,4'-diglucoside; 30 wt. % to 70 wt. % of the total flavonols of said extract consist of quercetin-3-monoglucoside and quercetin-4'-monoglucoside; and 20 wt. % to 30 wt. % of the total flavonols of said extract consist of quercetin, for making a composition to control weight gain.
US20090054405 PI3 kinase modulators and methods of use The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, X, R1 and R2 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
WO2014055548A1 Anti-fibrotic pyridinones Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
CN103330210A Food resisting to secondary gout The invention provides food resisting to secondary gout. Every 15 g of such food contains 2-6 g of purified fine konjac flour, 1,000-1,500 mg of vitamin C and 8-12 g of ultrafine Gorgon fruit flour; flavoring additives, such as sweetening agents (stevioside, maltitol and erythritol) and a flavor agent (fruit essence), can also be added to the food. The gout symptom can be relieved remarkably 5-8 later after the food is eaten, and the food doesn't have any side effect to a human body.
CN102166224A Antibiotic mate for treating colibacillosis and preparation method thereof The invention relates to an antibiotic mate for treating colibacillosis and a preparation method thereof. The antibiotic mate comprises ingredients of flunixin meglumine, sodium hydrogensulfite and a solvent; and the mass ratio of the flunixin meglumine to the sodium hydrogensulfite to the solvent is (1-5):(0.1-0.2):100. The preparation method of the antibiotic mate comprises the steps of heating partial solvent to 50-60 DEG C; adding the sodium hydrogensulfite; stirring for dissolving; and then adding the flunixin meglumine; stirring for 5 minutes to dissolve the flunixin meglumine; regulating a pH value to be 8.5 by using triethanolamine; and adding partial solvent again. The antibiotic mate provided by the invention has the advantages of simplicity and convenience for preparation and low cost, has a better treatment effect while used together with an antibiotic treatment method of poultry colibacillosis, is beneficial to healthy growth of live stock and brings very good benefits to raising households.
US8008501 Inhibit the Immunoglobulin E (IgE) receptor signaling cascade; associated with mast and/or basophil cell degranulation such as allergic diseases, scarring, inflammation; e.g. 5-Methyl-3-phenyl-4-isoxazolecarboxylic acid, 2-methyl-4-quinolinyl Ester The present invention provides quinoline compounds that inhibit the IgE receptor signaling cascade that leads to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE receptor signaling cascade.
WO2006095014A1 2- (4-0x0-4h-quinaz0lin-3-yl) acetamides and their use as vasopressin v3 antagonists The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
CN103313608A Agent for improving milk yield and/or milk quality of ruminants, preventive or therapeutic agent for perinatal disease, and agent for improving reproductive efficiency The present invention addresses the problem of improving the milk yield and/or milk quality of ruminants for milk production, preventing or treating a perinatal disease of ruminants, and improving the reproductive efficiency of ruminants. The agent for improving milk yield and/or milk quality of ruminants,is characterized by containing cashew nut shell oil, heat-treated cashew nut shell oil, anacardic acid, cardanol, and/or cardol. The preventive or therapeutic agent for perinatal disease of ruminants, is characterized by containing cashew nut shell oil, heat-treated cashew nut shell oil, anacardic acid, cardanol, and/or cardol. The agent for improving reproductive efficiency of ruminants, is characterized by containing cashew nut shell oil, heat-treated cashew nut shell oil, anacardic acid, cardanol, and/or cardol.
EP1577302A1 Novel ethylenediamine derivatives A compound represented by the following formula (1): Q1-Q2-To-N(R1)-Q3-N(R2)-T1-Q4 [wherein, R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may have a substituent, or the like; Q2 is a single bond or the like; Q3 represents the following group: -C(R3a)(R4a)-{C(R3b)(R4b)}m1-{C(R3c)(R4c)}m2-{C(R3d)(R4d)}m3-{C(R3e)(R4e)}m4-C(R3f)(R4f)- (in which, R3a to R4e represent hydrogen or the like); T0 represents a carbonyl group or the like; and T1 represents -COCONR- or the like]; or salt thereof, solvate thereof, or N-oxide thereof. The compound is useful as a preventive and/or therapeutic agent for cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
WO2008063099A1 Agent and method for preventing and treating intoxication by alcohol-containing liquids and alcohol substitutes The invention relates to medicine and can be used for developing agents and methods to be used in toxicological practice and by population at home for preventing and reducing risks of dangerous diseases such as intoxication by alcohol substitutes and toxic components of alcoholic beverages. The invention is based on the use of known chemical compounds in the form of vicinal dithioglycoles. They are used for new purposes, namely for developing medicinal agents, the properties of which make it possible to prevent, treat or reduce speed of pathological processes generated by alcohol substitute intoxication. The inventive agents reduce or block the pharmacological effects of alcohols and the derivatives thereof, i.e. produce a direct effect on pathogenetic mechanisms of intoxication development. Said agents are most efficient when perorally administered. Experimental data items proving that the inventive agents and the preventing method, which consists in taking the agents before and after drinking low-quality alcohol-containing beverages and alcohol substitutes, can be widely used in future are also disclosed. The use of the invention makes it possible to reduce the number of intoxication cases produced by substitutes, to decrease the severity of intoxication and the toxic effect of alcoholic beverages consumed at home.
US20110038809 Growth control of oral and superficial microorganisms using gallium compounds The present invention provides methods for treating or preventing diseases and disorders caused by iron-dependent pathogenic microorganisms, such as bacteria, fungi, and parasites, by applying a gallium compound to an affected area. In particular, the present invention provides methods for treating or preventing dental caries, vaginal infections, skin infections, and so forth. Gallium compounds can be formulated as toothpaste, mouthwash, cream, ointment, gel, solution, eye drops, suppository, and the like. Furthermore, the invention provides methods for controlling microbial growth on environmental surfaces, including those of toothbrush, denture, dental retainer, contact lens, catheter, food stuff, and so forth. In addition, the present invention provides animal feeds which contain gallium compounds that promote the animal growth and prevent the animals from infections as well as protect consumers from post processing infections.
WO2008058449A1 Pyrroline-2-one derivatives against cell releasing tumor necrosis factor, preparation methods and uses thereof Compounds represented by formula (I) or (II) against cell releasing TNF α, their pharmaceutically acceptable salts or hydrates and preparation methods and uses thereof, in which A, B and E represent CH2, CO respectively; D represents S, NH, NC1-6 alkyl; R represents H, R3 ; R1 represents 1-4 same or different radical(s) selected from the group consisting of F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2; R2 represents F, CF3, H or C1-4 alkyl.
US20050118157 Treatment of central nervous system damage The invention provides a method of promoting neuronal plasticity in the CNS of a mammal, the method comprising administering to the CNS of the mammal an agent that reduces the inhibitory properties of chondroitin sulphate proteoglycans. Preferred agents are chondroitinases and sulfatases, e.g., chondroitinase ABC. Also provided are methods of identifying further agents.
US20060029623 Invert emulsions comprising at least one active agent sensitive to water and cosmetic/dermatological applications thereof Cosmetic/dermatological compositions useful for the treatment of a variety of dermatological conditions, including keratinization disorders, acne, eczema, psoriasis, etc., comprise an invert emulsion containing at least one active agent sensitive to the presence of water, notably a derivative of vitamin D, and solubilized in a glycolic or hydroglycolic dispersed hydrophilic phase, a lipophilic continuous phase and an emulsifier having an HLB ranging from 2 to 7; these invert emulsions exhibit good stability and avoid crystallization of the active agent and/or chemical degradation thereof.
WO2014022237A1 Amorphous cabazitaxel The present invention is directed to an amorphous form of cabazitaxel, which can be prepared by dissolving a solid form of cabazitaxel in an organic solvent, and removing the organic solvent to dryness. The amorphous form of cabazitaxel is characterized by DSC as in FIG. 1 and/or X-ray powder diffraction pattern as in FIG. 2.
CN103193838A Etimicin sulfate pseudo-polymorph, and preparation method and application thereof The invention discloses an etimicin sulfate pseudo-polymorph, and a preparation method and an application thereof. The X-ray powder diffraction pattern of the pseudo-polymorph has characteristic peaks appearing at 2theta having degrees of 5.1+/-0.2, 6.0+/-0.2, 7.0+/-0.2, 7.6+/-0.2, 8.5+/-0.2, 10.9+/-0.2, 12.5+/-0.2, 13.1+/-0.2, 13.7+/-0.2, 15.5+/-0.2, 16.0+/-0.2, 16.6+/-0.2, 17.2+/-0.2, 17.6+/-0.2, 19.4+/-0.2, 19.9+/-0.2, 20.1+/-0.2, 20.5+/-0.2, 21.7+/-0.2, 22.6+/-0.2, 23.2+/-0.2, 24.0+/-0.2, 24.5+/-0.2, 26.0+/-0.2, 26.7+/-0.2, 27.1+/-0.2, 27.6+/-0.2, 28.4+/-0.2 and 28.8+/-0.2. The invention also discloses the preparation method of the pseudo-polymorph, and the application of the pseudo-polymorph in the preparation of medicines for treating human bacterial infectious diseases.
EP2421520A1 Pharmaceutical compositions for the treatment of nasal polyposis The present invention relates to osmotic agents for use in treating nasal polyposis and to pharmaceutical compositions containing thereof.
WO2009052090A3 Silicate containing compositions and methods of treatment The present invention relates to compositions comprising a silicate and methods of use thereof. In particular, the compositions of the present invention are suitable for treating inflammatory conditions, cancer, bacterial and viral infections, and infected and uninfected wounds. The compositions of the present invention can also be useful in treating spinal cord injury, tissue remodeling, and promoting bone growth and repair.
CN102920650A Carnosic acid solid dispersion and preparation method thereof The invention discloses a carnosic acid solid dispersion and a preparation method thereof. The carnosic acid solid dispersion can obviously improve the digesting performance and oral bioavailability of the carnosic acid. The carnosic acid solid dispersion is composed of carnosic acid raw materials and a carrier material, the mass ratio of the carnosic acid raw materials to the carrier materials is 1: (2-10), the mass ratio of the carnosic acid in the carnosic acid raw materials is 20%-100%, and the carrier material is at least one of povidone and poloxamer. The preparation method sequentially includes the steps of preparing the an organic solvent solution of the carnosic acid raw materials and the carrier material, mixing the solution, wherein the organic solvent is one of absolute ethyl alcohol, 95% of ethanol, acetone and ethyl acetate; and performing vacuum drying or spray drying to remove the organic solvent to obtain the carnosic acid solid dispersion.
CN101601690A Preparation method of soup for quickly loosening bowels The invention discloses a preparation method of a soup for quickly loosening bowels. The bowels can be quickly loosened within hours by using the method. The method is realized by adopting the following technical scheme that: honey is put in a porcelain, then the porcelain stored with the honey is loaded in a food steamer to be steamed for 30-90 minutes at 7-90 DEG C, natrii sulfas is finely ground, the boiling soup is well blended, then the honey, the natrii sulfas and the boiling soup are mixed together to be stirred for 5-10 minutes and then heated for 10-20 minutes after 30 minutes, and then the fire is stopped to obtain the finished medical soup at the cool temperature.
EP1411960B1 Fortified rice bran food product for promoting cardiovascular health A fortified rice bran food product for preventing and/or treating cardiovascular disease in animals, contains in admixture: (a) rice bran as a carrier; (b) at least about 12.5 milligrams of vitamin B1 per 30 grams of the rice bran; (c) at least about 250 milligrams of vitamin C per 30 grams of the rice bran; (d) at least about 12.5 milligrams of vitamin B6 per 30 grams of the rice bran; (e) at least about 75 micrograms of vitamin B12 per 30 grams of the rice bran; (f) at least about 100 International Units of vitamin E per 30 grams of the rice bran; (g) at least about 0.25 milligrams of folic acid per 30 grams of the rice bran; and (h) at least about 250 milligrams of omega-3-fatty acids per 30 grams of the rice bran. A method for preventing and/or treating cardiovascular disease in an animal involves orally administering a therapeutically effective amount of the fortified rice bran food product to the animal for a therapeutically effective period of time.
US20100247607 Implantable formulations of bisphosphonic acids The invention relates to devices, methods and formulation for subcutaneous administration of a bisphosphonate. In such a device, a drug core, comprising a bisphosphonate, is disposed in a tube. The devices may be administered to a patient in need of subcutaneously wherein the release of the bisphosphonate is desired to provide sustained release of a therapeutically effective dose of the bisphosphonate.
CN101967164A Ruthenium (II) complex, preparation method thereof and application thereof to preparation of antitumor medicaments The invention discloses a ruthenium (II) complex, a preparation method thereof and application thereof to preparation of antitumor medicaments. The ruthenium (II) complex has a structural formula shown as a formula (I), wherein X is thiophene or indol; and N-N is bipyridyl, biimidazole or phenanthroline. The ruthenium (II) complex does not comprise readily hydrolytic chlorine (Cl) or dimethylsulfoxide (DMSO) structurally. Compared with the traditional ruthenium complex, the ruthenium (II) complex has the advantages of obviously enhancing stability, reducing toxicity and obviously improving antitumor activity, so the ruthenium (II) complex can be used for preparing medicaments for preventing or treating tumor diseases.
CA2402635C Method for oxidizing a thioether group into a sulfoxide group The present invention relates to a process for the oxidation of the compound 2-(2-pyridinylmethyl-thio)benzimidazol of formula I to the compound of formula II, characterized in that the oxidation is effected with sodium percarbonate and a catalyst consisting of a molybdenum salt (see formula I) where R1 represents an alkyl group with 1 to 6 carbon atoms, a halogenated alkyl group with 1 to 6 carbon atoms or a -(CH2)n-OR9 group, where n is an integer between 1 and 6, both inclusive, and R9 represents hydrogen or an alkyl group with 1 to 6 carbon atoms; R2, R3, R4, R5, R6 and R9, independently from each other represent hydrogen, an alkyl group with 1 to 6 carbon atoms or an alkoxy group with 1 to 6 carbon atoms; and R7 represents hydrogen, an alkyl group with 1 to 6 carbon atoms, an alkoxy group with 1 to 6 carbon atoms or a fluorinated alkoxy group with 1 to 6 carbon atoms.
EP2345654A1 Eszopiclone particles and a process for their preparation The present invention provides crystalline eszopiclone having particles in the shape of sticks that enables process for the preparation of pharmaceutical composition without segregation of drug substance. Further, the present invention provides the process for preparing crystalline eszopiclone having particles in the shape of sticks.
CN102648898A Method for preventing azithromycin from adhering during tabletting The invention provides a method for preventing azithromycin from adhering during tabletting. The method comprises the following steps: (1), azithromycin and dispersant are pulverized and sieved with a 80-mesh sieve respectively; (2), azithromycin and dispersant, which are obtained in step (1), are mixed completely and then filled in an airflow pulverizer to be pulverized in an ultramicro manner; (3), powder obtained in step (2) is sieved with a 120-mesh sieve, so that a ultramicro pulverized mixture of azithromycin and dispersant is obtained; and (4), the ultramicro pulverized mixture obtained in step (3) is mixed with one or more of loading agents, disintegrating agents, lubricant, bonding agents, glidant and flavoring agents, and then tabletting is performed, wherein the dispersant is one of microcrystalline cellulose and kaolinite, and the use amount of the dispersant is 2 to 10 times of the weight of azithromycin by the basic group. The invention effectively overcomes the phenomenon that azithromycin adheres during the tabletting process.
WO2008080968A1 Freeze-dried injectable pharmaceutical combination of semisynthetic vinca alkaloids and carbohydrate stable at room temperature This invention relates to pharmaceutical compositions consisting of a semisynthetic derivative of vinca alkaloid, stable at room temperature, in which said derivative is present in the form of a freeze dried product obtained in the presence of at least one carbohydrate.
WO2013108262A1 Synergistic combination for the treatment of diabetic neuropathy This invention is based on an efficient treatment of diabetic neurotherapy. The drug combination is made up three ingredients. These are taurine, folic acid and methylcobalamin. These are working as a synergistic compound for the treatment of diabetic neurotherapy the concentration of these compounds are Methylcobalamin is 1500 microgram per tablet, taurine is 500 mg per tablet and folic acid is 5 mg per tablet. In this combination taurine is used for anxiolytic effect and may act as a modulator or anti- anxiety agent in the central nervous system. Folic acid is used for the mechanism of blood glucose control. It is essential because glucose causes high levels of oxidative stress throughout the body. In antioxidant therapy folic acid is very important antioxidant to help prevent neuropathy and Methylcobalamin is used in the treatment of diabetic neuropathy, it is a form of vitamin B12. Methylcobalamin are necessary to correct neurological defects. This combination can provide relief in infections on the feet and legs, in multiple fractures of the knee, ankle or foot, a Charcot joint as well as loss of motor function resulting in dorsiflexion, contractures of the toes, loss of the interosseous muscle function and contraction of the digits, so called hammer toes, loss of the musculature making the hand appear gaunt and skeletal and the loss of muscular function.
CN101829129B Veterinary compound gentamycin sulfate injection and preparation method thereof The invention relates to a veterinary compound gentamycin sulfate injection and a preparation method thereof. The injection consists of gentamicin sulphate, ofloxacin, analgin, trimethoprim, an organic solvent and injection water. The injection serving as a veterinary special compound preparation is mainly used for treating porcine epidemic diarrhea, transmissible gastrocnteritis, paratyphus vaccine for piglets, yellow and white scour for piglets, edema disease for piglets, and intestinal diseases, such as poultry colibacillosis, fowl typhoid, paratyphoid and the like. The injection has the advantages of convenient use, short period of treatment, low medicament resistance and the like.
EP2168440A1 Equol-containing extract, method for production thereof, method for extraction of equol, and equol-containing food The present invention relates to an extract obtained by extracting useful components containing equol from an equol-containing fermented soybean hypocotyl, and to a method for producing the same. The present invention makes it possible to efficiently obtain useful components containing equol from the fermented soybean hypocotyl by subjecting an equol-containing fermented soybean hypocotyl to extraction using an ethanol aqueous solution as an extractant. The present invention reduces the content of saponin, which causes an unpleasant taste, by sequentially subjecting the equol-containing fermented soybean hypocotyl to extraction using an ethanol aqueous solution and ethanol, while efficiently extracting equol and glycitein.
US7235634 Comprises proteolytic enzymes for use as tools to identify modulators for treatment and prevention of gastrointestinal, cell proliferative and inflammatory diseases The present invention relates to a newly identified human aminopeptidase. The invention also relates to polynucleotides encoding the aminopeptidase. The invention further relates to methods using the aminopeptidase polypeptides and polynucleotides as a target for diagnosis and treatment in aminopeptidase-related disorders. The invention further relates to drug-screening methods using the aminopeptidase polypeptides and polynucleotides to identify agonists and antagonists for diagnosis and treatment. The invention further encompasses agonists and antagonists based on the aminopeptidase polypeptides and polynucleotides. The invention further relates to procedures for producing the aminopeptidase polypeptides and polynucleotides.
US20110212076 Viral Therapeutic The invention provides a method of inhibiting viral infection of a mammalian cell, said method comprising reducing or inhibiting ps20 polypeptide expressed by said cell. Suitably ps20 is inhibited by contacting said cell with an antibody capable of binding to ps20 polypeptide. Suitably said antibody is ps20 neutralising antibody. The invention also provides antibody capable of binding ps20 polypeptide, siRNA targeted to a transcript encoding ps20 polypeptide, or antisense ps20 polynucleotide for use as a medicament for viral infection. The invention also provides a method of identifying an agent for inhibiting a viral infection, comprising determining level of ps20 expression in first and second samples, the first contacted with test agent; and comparing the level of ps20 expression in said first and second samples; wherein lower level of ps20 expression in said first sample relative to said second sample identifies test agent as an agent for inhibiting a viral infection.
CN1772197A Prepn process of micron Yin-nourishing hypoglycemic medicine granule, capsule and tablet The present invention relates to the preparation process of micron Yin-nourishing hypoglycemic medicine granule, capsule and tablet. The Yin-nourishing hypoglycemic medicine granule, capsule and tablet consist of micron level ginseng whisker powder, micron level American ginseng powder, micron level asparagus root powder, micron level wolfberry fruit powder, micron level sealwort powder, micron level chromium amide powder, propolis and xylitol. It has obvious functions of nourishing Yin, reducing blood sugar, strengthening immunity, etc. The present invention makes it possible for the old people and middle aged people to obtain hundreds nutritious matters, including rich protein, vitamins, minerals, etc.
US20100015218 Compositions and methods for potentiated activity of biologically active molecules The present invention relates to novel compositions and methods for potentiating the activity of biologically active molecules in conjunction with one or more delivery vehicles and one or more carrier molecules. Specifically, the invention features the use of a carrier molecule in combination with a delivery vehicle and a biologically active molecule of interest to potentiate the activity of the biologically active molecule. The carrier molecule can be biologically inert, inactive, or attenuated; or can alternately be biologically active in the same or different manner than the biologically active molecule of interest. Specifically, the invention features novel particle forming delivery agents including cationic lipids, microparticles, and nanoparticles that are useful for delivering various biologically active molecules to cells in conjunction with a carrier molecule. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism that are delivered intracellularly in conjunction with a carrier molecule. In various embodiments, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules, to relevant cells and/or tissues, such as in a subject or organism, in conjunction with one or more carrier molecules. Such novel cationic lipids, microparticles, nanoparticles and transfection agents that are used in conjunction with one or more carrier molecules are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism.
CN103393767A Garlic reaction activin The invention provides garlic reaction activin. The garlic reaction activin comprises peppermint, honeysuckle, plantain herb and ammonium salt. Raw materials can also comprise trollflower and cauda equine which is rolled into flour after being stir-fried. The garlic reaction activin provided by the invention, the formula of the garlic reaction activin is simple, and is matched with pasty mashed garlic for use, so that garlic molecules can be rapidly and effectively released, and the utilization rate of the garlic is increased. The released garlic gas directly acts on the lung of a human body and has a very god treatment effect on lung diseases and a very good adjuvant therapy effect on tumors.
US20100068307 Dermatological emulsion and method for the preparation thereof A foaming gelled composition in the form of a stable oil-in-water microemulsion comprising a fatty phase of microdroplets dispersed in an aqueous phase and a dermatological active ingredient, characterized in that it comprises a surfactant system comprising:—at least one ethoxylated nonionic surfactant;—at least one cosurfactant for stabilizing the ethoxylated nonionic surfactant;—at least one nonethoxylated hydrophilic nonionic surfactant;—at least one foaming agent chosen from the group of anionic surfactants.
CN101407557A Preparation and use of Dendrobium nobile polysaccharide extract The invention provides a preparation method of dendrobium nobile polysaccharide extracts, which is realized by steps of degreasing, extracting, alcohol precipitating, protein removing, monose and oligosaccharide removing and purifying gel columns and the like. The polysaccharide content in the polysaccharide extract is more than 93 percent. The polysaccharide extract has remarkable oxidation prevention activity, can be combined with medicament excipients and carriers permitted by preparation agents, and can be applied in preparing medicaments or medicament combinations for treating and preventing cardiovascular diseases. The preparation method of the dendrobium nobile polysaccharide extracts is reasonable in design and convenient in operation.
US7375106 Analgesic; Ketorolac or indomethacin nsaid with an opioid diarylmethyl piperazine such as 3-[( alpha R)- alpha -((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl]-N-(3-fluorophenyl)-N-methylbenzamide; dosage of the opioid can be decreased so side effects are reduced The invention relates to a combined pharmaceutical preparation comprising an opioid diarylmethyl piperazine compounds and a NSAID. Such a preparation in which the compounds are either given sequentially or simultaneously can be used for the treatment of pain diminishing the side-effects observed in conventional opioid treatments.
CN102861001A Novel application of cinnamic aldehyde for treating gastritis The invention discloses a novel application of cinnamic aldehyde in a gastritis treatment medicine. According to the novel application of the cinnamic aldehyde in the gastritis treatment medicine, the production cost is low, the efficacy is high, the dosage and the toxic effect are small, and the defects that common gastritis treatment medicines have big side effect and long treatment course and the like are overcome. The cinnamic aldehyde can be applied to preparation of the gastritis treatment medicine. The cinnamic aldehyde can be prepared to be pharmaceutically acceptable dosage forms of tablets, sustained-release tablets, capsules and injections and the like. The novel application of the cinnamic aldehyde in the gastritis treatment medicine has a wide applying prospect in the aspect of medical health care.
US20080287539 Use of carnitines for the prevention and/or treatment of disorders caused by the andropause L-carnitine, propionyl L-carnitine and/or acetyl L-carnitine are used to prevent or treat disorders of male andropause caused by ageing or by chemical or surgical castration.
WO2010065709A3 Hydroxamic acid derivatives, preparation and therapeutic uses thereof Disclosed are amino alkyl/aryl hydroxamic acid compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for degenerative diseases in mammal.
US20090281174 Senescence inhibitor Provision of a drug, a quasi-drug, and a food or beverage, which are effective for senescence inhibition, mitochondrial function improvement, muscle dysfunction inhibition, muscular atrophy inhibition, prevention of a bedridden state, muscle senescence inhibition, or motor function improvement. A senescence inhibitor, a mitochondrial function-improving agent, a muscle dysfunction inhibitor, a muscular atrophy inhibitor, and an agent for preventing a bedridden state, containing a catechin as an effective ingredient. A muscle senescence inhibitor and a motor function-improving agent, containing a catechin and an amino acid as effective ingredients.
US20110243959 Modulating neuronal plasticity and treatment of neuronal loss by modulationg wnt7a or wnt7b modulation The present invention relates to a method of treating or preventing a disease characterized by a loss or imbalance of neuronal connections, wherein said disease characterized by a loss or imbalance of neuronal connections is selected from a group of diseases consisting of age-related loss of neuronal performance and/or connections, psychiatric disorders, neurodegenerative diseases characterized by loss of neuronal connections, learning deficiency, and senile dementia, of modulating neuronal activity and/or neuronal plasticity, of optimizing repair after brain injury, to modulate learning, and/or to modulate cognitive capabilities, in a subject and/or, of preventing loss of neuronal connections and/or to increase neuronal connections in said subject, by modulating Wnt-signaling, which method is characterized by the fact that the subject is in puberty or post-puberty, wherein puberty or post-puberty means that the neuronal circuits of said subject have already undergone developmental synapse elimination and critical periods which take place prior to puberty.
EP2658545A1 Treatment of pain associated with dislocation of basal endometrium The present invention relates generally to gynecological diseases and in particular to a method for reducing pain associated with dislocation of basal endometrium.
WO2006039792A1 Method of treating autoimmune diseases The invention features a method of inducing an apoptosis-resistant cell to undergo apoptosis, in which the cell is associated with an autoimmune disease such as multiple sclerosis. The method involves sensitizing the cell to apoptosis stimuli by treating the cell with an IAP antisense oligonucleotide, so that the cell undergoes apoptosis at a site of autoimmune disease.
US7595394 Porphyrin compound, albumin inclusion compound thereof and artificial oxygen carrier A porphyrin compound represented by general formula (A): Also disclosed are a porphyrin metal complex-albumin inclusion compound having a porphyrin compound, in which M denotes Fe or Co, included in albumin, and an artificial oxygen carrier containing the porphyrin metal complex-albumin inclusion compound as an active component.
CN101904831A Application of alkannin and compositions thereof The invention discloses application of alkannin and compositions thereof in preparing medicaments for preventing and treating vessel and local tissue injury caused by extravasation of chemotherapeutic agents. The rat in-vivo pharmacological research and clinical research show that the alkannin has obvious effects of treating the vessel and local tissue injury caused by extravasation of chemotherapeutic agents and promoting healing and can obviously shorten the time of eliminating the swelling of the local tissues and accelerate the healing of the local tissue injury, and also show that the alkannin and compositions thereof can be used for preparing the medicaments for preventing and treating the vessel and local tissue injury caused by the extravasation of the chemotherapeutic agents.
CN1994308A Pain-relieving medicinal ointment The invention relates to a painkiller paste used to release local ache of muscle, wherein it comprises adeps lanae, camphoric acid and betula oil. The invention can avoid oral intake, but external coat.
US20050214384 Chromium compositions and methods for using the same for inhibiting drug-induced insulin resistance A method for inhibiting drug-induced insulin resistance is provided which includes administering a dietary chromium complex to an individual receiving a contemporaneous dose of a drug that induces insulin resistance, wherein the amount of chromium complex administered is an amount effective to inhibit the development of insulin resistance. Advantageously, the amount of chromium complex administered per day is between about 300 and 1,000 micrograms per day. Compositions including a drug which induces insulin resistance in combination with a chromium complex are similarly described.
WO2011015728A1 Novel dihydroindolone derivatives, process for the preparation thereof and pharmaceutical compositions containing same Compounds of the formula (I) in which: m and n are 1 or 2, A is a pyrrolyl group, X is the group C(O), S(O) or SO2, R1 and R2 are an alkyl group, or together form, with the nitrogen atom which bears them, a heterocyclic group, R3 and R4 together form, with the atoms which bear them, a heterocyclic group, R5 is a hydrogen atom or an alkyl group, and R6 is a hydrogen atom or a halogen atom. Medicaments.
CN1965850B Roxithromycin injection and preparation process thereof The invention relates to an eritrocina injection, wherein the invention has high solubility, used in vein injection. The eritrocina and aspartic acid will react in water and room temperature to generate soluble salt, while they react in equal mol number; the injection contains 50-500mg eritrocina, and the solution can be made into injection or powder via added supporter. The invention has quick drug release, high stability and quick treatment.
EP1461025B1 Treatment of parkinson's disease with cape A method of treating a neurodegenerative or cardiovascular disorder with a compound of the following formula (I): in which X, Y, A1, A2, R1 and R2 are defined herein.
US20120178767 Treatment of liver disorders with p13k inhibitors The invention provides methods to treat certain liver disorders by administering a compound that inhibits PD K isoforms, particularly the delta isoform. It further provides specific compounds useful for these methods and ways to identify subjects who are particularly suitable for receiving these treatments.
US20070299132 Stable Aqueous Formulation of a Platin Derivative Disclosed is a stable aqueous formulation of a platin derivative, particularly oxaliplatin. The selected stabilizing additive is effective even in very small concentrations.
CN102361640A Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids A method for treating a subject having an inflammatory or auto-immune disease with a substituted isoxazolo pyridinone. Also, a method for administering a substituted isoxazolo pyridinone to a cell to retain or increase glucocorticoid receptor transrepression activity with only minimal glucocorticoid receptor transactivation activity.
WO2014159054A1 Gpr120 agonists for the treatment of type ii diabetes Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: Formula (I) wherein Y, R1, G, and Q are defined herein; and Formula (II) wherein R11, R21, R41, RB1 and G1, are defined herein.
WO2008056176A1 Pyrazolopyrimidines as phosphodiesterase inhibitors Compounds for use as phosphodiesterase inhibitors, and in particular for inhibiting PDE 11. The compounds may be used in therapy or as a medicament in the treatment of, for example, schizophrenia.
CN103142477A Preparation method of sustained-release colchicine micro emulsion preparation containing nanometer-carrier The invention provides a sustained-release colchicine micro emulsion preparation containing nano-hydroxyapatite. The sustained-release colchicine micro emulsion preparation containing the nano-hydroxyapatite comprises a calcium phosphate solution containing the colchicine, oil phase, a surfactant and a cosurfactant. The nano-hydroxyapatite is used for medicine carrying sustained release, the medicine carrying capacity is increased, medicine is released out at a relatively constant controllable speed, and therefore the number of times of dressing change is reduced.
CN103214447A Liparis nervosa extract monomeric compound as well as preparation method and application thereof The invention provides Liparis nervosa extract monomers with a common parent nucleus and application of the Liparis nervosa extract monomers to antipyresis, anti-inflammation and analgesia, wherein the application is confirmed through pharmacological experiments. The invention provides two Liparis nervosa extract monomers. The method is simple in process; monomers with purity greater than or equal to 95% are obtained; and the two monomers have favorable activities in the aspects of antipyresis, anti-inflammation and analgesia.
WO2011024049A3 Method for producing proanthocyanidin polymer compositions for pharmaceutical formulations Processes for producing pharmaceutical compositions containing a proanthocyanidin polymer useful for the treatment and prevention of various conditions are provided. The invention specifically relates to processes for producing pharmaceutical formulations of a proanthocyanidin polymer composition which has been isolated from a Croton spp. or a Calophyllum spp. In particular, the invention relates to a process for producing proanthocyanidin polymer compositions which achieve concentrations and purities useful for addition to pharmaceutically effective formulations.
US20080096894 Anti-Bacterial Compounds Compounds of formula (I), or salts or solvates thereof, in vitro as inhibitors of growth of Gram-positive bacteria, where A is selected from formula (a).
US20090099221 Pyridyl-and pyrimidinyl-substituted pyrrole-, thiophene-and furane-derivatives as kinase inhibitors The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer
CN1883531A A medicinal powder with climbing groundsel for treating hicismus The invention provides a medicinal powder for treating body odor which is prepared from the following raw materials (by weight ratio): Senecio scandens, white charcoal, clove, clamshell powder, buthus martensi kirsch and boneol, and the preparing process comprises the steps of sieving and mixing powders of each constituents.
CN103479659A Application of three kinds of oroxin in preparing drug for resisting staphylococcus aureus infection The invention relates to application of three kinds of oroxin in preparing a drug for resisting staphylococcus aureus infection. The staphylococcus aureus infection resistance of three kinds of oroxin can be proved by virtue of a sheep red blood cell haemolysis test, molecular dynamics simulation and a human pulmonary epithelial cell (A549) injury protective test. Compared with treatment by antibiotics, treatment by using three kinds of oroxin has the characteristics of no drug resistance and high cure rate, so that the three kinds of oroxin can be used in development of new drugs, and has an important meaning to drug target confirmation.
CN1796393A Analogue of nucleotide This invention describes the prodrug of a phosphoromethoxyl nucleic acid analogue containing pentacyclic triterpenoid compounds and its preparation process. The prodrug has anti-AIDS and anti-Hepatitis B virus activity as well as liver-protecting function, and can be used to prepare drugs.
US20090076166 Enterically coated cystamine, cysteamine and derivatives thereof 8 The disclosure provides oral cysteamine and cystamine formulations useful for treating cystinosis and neurodegenerative diseases and disorders. The formulations provide controlled release compositions that improve quality of life and reduced side-effects.
CN101693103A Improvement of completeness of intestinal barrier The invention relates to an improvement of completeness of an intestinal barrier, in particular to a method for exciting the barrier completeness of mammalian by applying a composition containing eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA) and arachidonic acid (ARA) and at least two different oligosaccharides to the mammalians.
WO2009126606A2 Regression of established atherosclerotic plaques, and treating sudden-onset asthma attacks, using parp inhibitors A method is disclosed for treating and inducing the regression of established atherosclerotic plaques. A method is disclosed fortreating asthma, including treatment of an ongoing asthma attack. In both cases, treatment with PARP inhibitors, such as the PARP inhibitor TIQ-A (Thieno[2,3-c]isoquinolin-5-one), can lead to regression of existing disease and symptoms.
CN101927004A Macromolecule slow controlled release long-acting sterilizing product and preparation method thereof The invention relates to a macromolecule slow controlled release long-acting sterilizing product and a preparation method thereof. The macromolecule slow controlled release long-acting sterilizing product comprises the following components: 0-30 percent of alcohol, 0.05-2.5 percent of polyvinyl pyrrolidone, 0-2.0 percent of polyquaternium, 0-3.0 percent of macromolecule acrylate copolymer, 0.3-5.0 percent of sodium laureth sulfate, 0-3 percent of cocoamidopropyl betaine, 0-3.0 percent of colza oil polyoxyethylene amide, 0-3.0 percent of lauryl sulfate triethanolamine salt, 0-6.0 percent of glycerol, 0-3.0 percent of propylene glycol, 0-2.5 percent of natrosol, 0-2.0 percent of dimethyl siloxane polyether, 0-1.2 percent of methyl-p-hydroxy benzoate, 0-1 percent of propylparaben, 0-15 percent of chlorhexidine gluconate solution (20 percent), 0-10 percent of glutaraldehyde (or combined with other sterilizing components), 0-0.1 percent of tea tree oil, 0.02-0.8 percent of perfume, 0-2.5 percent of sodium chloride and the balance of deionized water. The product can have the effects of durably sterilizing and nourishing the skin, and can be used for continuously sterilizing for several hours on the surface of the skin and continuously sterilizing several days on the surface of an object.
US20080075719 Method for Augmenting B Cell Depletion The present invention provides methods of augmenting B cell depletion by promoting intravascular access of B cell subsets sequestered in lymphoid tissues rendering the B cells sensitive to killing mediated by the B cell depleting agent. One method of promoting intravascular access is by the use of integrin antagonists. Methods of treating B cell disorders by this approach is also provided.
DE102005045989A1 Powder base, useful for e.g. protecting the skin from disorders, comprises e.g. protective material, mineral pigment, different organic materials, urea, antimicrobial-, antiseptic-, anitinflammatory- and itch protective- agents Powder base (C1), for protecting the skin from skin barrier disorders and Corn's disease, partially or completely from UV light and for disorders in wounded and tinged skin and in healthy skin, comprises protective material (99.99-97 wt.%), mineral pigment, different organic materials, urea (0.01-3, preferably 0.1-1 wt.%), antimicrobial-, antiseptic-, antiinflammatory- and itch protective- agents, radical inhibitors, and does not contain allergic and irritative components. An independent claim is also included for a medicinal powder comprising (C1) with a pharmaceutical active substance (0.01-2, preferably 0.1-1 wt.%) such as vitamin, local anesthetics, H1-antihistaminic, antimycotic, antiinflammatory active agents, immunosuppressive, antiinfective, antiseptic, static virus, astringents, barrier stabilizing agent or protein hydrolysate condensate. - ACTIVITY : Dermatological; Vulnerary. No biological data given. - MECHANISM OF ACTION : None given.
US20130018039 Imidazolyl-imidazoles as kinase inhibitors Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are defined herein, and methods of making and using the same.
US20090041877 Composition comprising growth factor of xanthoceras sorbifolia extracts, compounds isolated from same, methods for preparing same and uses thereof This invention provides a process of producing extract comprises growth-stimulation components from husks, kernels, leaves, fruit-stems, branches, stems, roots, seed's shells and barks and their applications. A use of composition comprising the extract from the husks, kernels, leaves, fruit-stems, branches, stems, roots, seed's shells and barks of Wenguanguo for stimulating the cell activities comprising growth-stimulation by administering an appropriate amount of the above composition.
CN102397249A Cefetamet pivoxil hydrochloride liposome solid preparation The invention provides a cefetamet pivoxil hydrochloride liposome solid preparation and a preparation method thereof. The cefetamet pivoxil hydrochloride liposome solid preparation comprises 125 parts of cefetamet pivoxil hydrochloride, 20 to 250 parts of aluminum dicetyl phosphate, 50 to 200 parts of cholesterol, 10 to 150 parts of tween 80 and 100 to 250 parts of other medicinal auxiliary materials. The cefetamet pivoxil hydrochloride liposome solid preparation can be processed into tablets and particles. The cefetamet pivoxil hydrochloride liposome solid preparation has a high entrapment rate, even particle sizes and long retention time of drugs in blood circulation. The preparation method of the cefetamet pivoxil hydrochloride liposome solid preparation improves preparation quality, reduces toxic and side effects, needs simple equipment, is easy for operation and is suitable for industrialized large-scale production.
US6899888 Suppressing bone disordes such as decalcification or fractures in humans having prostate gland cancers by administering antiestrogen selected from triphenylethylene or toremifene; hormone inhibitors This invention provides: 1) a method of treating androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 2) a method of preventing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 3) a method of suppressing or inhibiting androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer; and 4) a method of reducing the risk of developing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer, by administering to the subject a pharmaceutical composition comprising an anti-estrogen agent and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein.
CN101040867A Application of fucoidan in the preparation of medicine and health-care products for preventing and treating neurodegenerative diseases The invention discloses a fucose sulfate or a compound whose active component is fucose sulfate, in the drug preparation on the treatment of nerve retrograde disease and cognition damage. And the invention discloses the relative application. The inventive fucose sulfate is mainly from marine invertebrate animal as sea-tangle, sea cucumber or the like, with wide resource, easy production, batch production, and wide application.
EP1192164B1 Thieno- and furopyrimidine derivatives as a2a-receptor antagonists A compound of formula (I) wherein X is O or S; R1 and R2 are independently selected from hydrogen, alkyl, aryl, hydroxy, alkoxy, aryloxy, cyano, nitro, CO2R7, COR7, OCOR7CONR7R8, CONR7NR8R9, OCONR7R8, NR7R8, NR7COR8, NR7CONR8R9, NR7CO2R8, NR7SO2R8, NR7CONR8NR9R10, NR7NR8CO2R9, NR7NR8CONR9R10, NR7SO2NR8R9, SO2R7, SOR7, SR7 and SO2NR7R8, or R1 and R2 together form a carbonyl group (C=O), an oxime group (C=NOR11), an imine group (C=NR11) or a hydrazone group (C=NNR11R12), or R1 and R2 together form a 5, 6 or 7 membered carbocyclic or heterocyclic ring; R3 is alkyl or aryl; R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl, halogen, hydroxy, nitro, cyano, alkoxy, aryloxy, COR7, OCOR7, CO2R7, SR7, SOR7, SO2R7, SO2NR7R8, CONR7R8, CONR7NR8R9, OCONR7R8, NR7R8, NR7COR8, NR7CONR8R9, NR7CO2R8, NR7SO2R8, CR7=NOR8, NR7CONR8NR9R10, NR7NR8CO2R9, NR7NR8CONR9R10, SO2NR7NR8R9, NR7SO2NR8R9, NR7NR8SO2R9, NR7NR8COR9, NR7NR8R9 and NR7CSNR8R9, or R5 and R6 together form a 5, 6 or 7 membered carbocyclic or heterocyclic ring; and R7, R8, R9, R10, R11 and R12 are independently selected from hydrogen, alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, and the use thereof in therapy, particularly in the therapy of a disorder in which the blocking of purine receptors may be beneficial, such as Parkinson's Disease.
US7592368 HIV aspartyl protease inhibitors; solubility, bioavailability; viral and HIV infections The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
WO2009019138A3 Enzymatic process for obtaining 17 alpha-monoesters of cortexolone and/or its 9,11-dehydroderivatives The present invention refers to an enzymatic process for obtaining 17alpha-monoesters of cortexolone and/or its 9, 11-dehydroderivatives starting from the corresponding 17alpha, 21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to crystalline forms of cortexolone 17alpha-propionate and 9,11-dehydro-cortexolone 17alpha-butanoate.
US20100240641 Aldosterone Synthase and/or 11B-hydroxylase Inhibitors The present invention provides a compound of formula I: Said compound is inhibitor of CYP11B2 and/or CYP11B1, and thus can be employed for the treatment of a disorder or disease mediated by CYP11B2 and/or CYP11B1.
CA2187162C Dna encoding precursor of interleukin-1.beta. converting enzyme-related cysteine proteinase iii (icerel iii) A complementary DNA (cDNA) encoding full length form of ICErel-III is identified, sequenced and isolated. The cDNA is cloned into expression vectors for expression in recombinant hosts. The cDNA is useful to produce recombinant full length ICErel-III. The cDNA and the recombinant ICErel-III protein derived therefrom are useful in diagnostic kits, laboratory reagents and assays. The cDNA and the recombinant ICErel-III protein may be used to identify compounds that affect ICErel-III function, inflammation and cell apoptosis. ICErel-III function, inflammation and cell apoptosis may also be modulated by ICErel-III antisense or gene therapy.
WO2005011665A1 The use of proglumide for the treatment of emesis Proglumide is useful for the treatment of a condition selected from nausea, dizziness, blurred vision and emesis. Such a condition may be druginduced.
WO2009103493A1 Sgk1 as a therapeutic and diagnostic target for viral diseases The invention relates to substances for diagnosing and treating viral diseases by using sgk1 (serum and glucocorticoid-dependent kinase 1) as a therapeutic and diagnostic target.
CA2335900C Aqueous compositions containing corticosteroids for nasal and pulmonary delivery The present invention provides compositions containing corticosteroid compounds as active agents for the treatment of ailments and diseases of the respiratory tract, particularly the lungs, by way of nasal and pulmonary administration. The corticosteroid compounds are present in a dissolved state in the compositions. The compositions can be formulated in a concentrated, essentially non-aqueous form for storage or in a diluted, aqueous-based form for ready delivery. In a preferred embodiment, the corticosteroid composition contains an ethoxylated derivative of vitamin E and/or a polyethylene glycol fatty acid ester as the high-HLB surfactant present in the formulation.The compositions are ideally suited for inhaled delivery with a nebulizer or for nasal delivery.
CA2338776C Novel c-2 s/o- and s/n formaldehyde acetal derivatives of carbapenem-3-carboxylic acids and their use as antibiotics and .beta.-lactamase inhibitors The compounds of general formula (I) wherein R1 denotes hydrogen, hydroxymethyl or 1-hydroxyethyl, R2 denotes hydrogen or methyl and R3 denotes a pharmaceutically acceptable group which is bonded to the remaining part of the molecule by an oxygen-carbon single bond or a nitrogen-carbon single bond, and their pharmaceutically acceptable salts, esters and amide derivatives are broad spectrum antibiotics and .beta.-lactamase inhibitors.
CN101602732A Derivative of acyl thiourea pyridine, method for preparing same and application thereof The invention relates to a thiourea compound, a method for preparing the same and application thereof, in particular to a derivative of acyl thiourea pyridine, a method for preparing the same and application thereof. The method comprises the following steps: using 2-amino-4-methyl pyridine as a raw material to synthesize a derivative of the 2-amino-4 substituted pyridine; reacting acyl chloride and potassium thiocyanate to obtain a coarse product of acyl isothiocyanate, and reacting the coarse product and the pyridine derivative to obtain the corresponding acyl thiourea pyridine compound. The derivative of the acyl thiourea pyridine prepared by the method has the actions of resisting the influenza virus activity, the hepatitis B virus activity and the oxidization and inhibiting the regeneration of vascular smooth muscles, so that the derivative of the acyl thiourea pyridine can be used for preparing medicaments of resisting the influenza virus activity, the hepatitis B virus activity and the oxidization and inhibiting the regeneration of the vascular smooth muscles.
WO2009019014A1 Novel benzimidazol-2-yl-alkylamines and the use thereof as microbicidal agents The present invention relates to novel benzimidazole-2-yl-alkylamines having antimicrobial properties, to methods for the production of said compounds, and the use thereof as microbicidal agents in pharmaceutical preparations or plant protectants. Although numerous microbicidal agents are known, the adaptability of microorganisms and thus the creation of resistance results in a continuous need for new, highly effective, but also physiologically sustainable substances with preferably new mechanisms of action and broader spectrums of activity. The described benzimidazol derivates of the following formula have a good antimicrobial effect, particularly against species of the genus candida. Toxicology tests have shown a good compatibility of the new agents. Two different methods are described for the production of the compounds. The compounds are used for the systemic and local treatment of humans, animals, and plants that are infected by harmful microorganisms, particularly fungi, bacteria, viruses, algae, protozoa, and other parasites (Formula I).
CA2850610A1 Sphingosine analogs, compositions, and methods related thereto The disclosure relates to compounds, pharmaceutical compositions, and methods of treating or preventing disease. In certain embodiments, the disclosure relates to methods of treating an infection or cancer comprising administering a pharmaceutical composition disclosed herein to a subject in need thereof. In a typical embodiment, one administers a pharmaceutical composition comprising sphingosine or a sphingosine analog to a subject at risk for, exhibiting symptoms of, or diagnosed with a malaria infection.
US20090118277 3 Unsubstituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidines as Kinase Inhibitors The invention relates to 3-unsubstituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidine compounds, their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.
CN103083281A Enteric-coated tilmicosin slow-release micro-capsule preparation and preparation method thereof The invention relates to an enteric-coated tilmicosin slow-release micro-capsule preparation and a preparation method thereof and belongs to the field of tilmicosin preparations. The enteric-coated tilmicosin slow-release micro-capsule preparation provided by the invention comprises an inner core layer and a coating layer, wherein the inner core layer comprises tilmicosin raw powder and an auxiliary material; the auxiliary material comprises one or more than one of stearic acid, glycerin monostearate, stearyl alcohol, saturated triglyceride, monoglyceride and paraffin; and the coating layer is made from one or more than one of cellulose acetate phthalate, hydroxypropyl methyl cellulose phthalate, acrylic resin, polyvinyl acetate phthalate and acetic hydroxypropyl methylcellulose succinate. The preparation method comprises the following steps of: carrying out primary coating on the tilmicosin raw powder and the auxiliary material, carrying out secondary coating by using the materials of the coating layer, and drying to obtain the finished product. According to the invention, the tilmicosin is coated by using high polymer materials and the coated tilmicosin micro-capsule is undissolved in acid environment and slowly dissolved in alkaline environment of enteric canal, so that the purpose of slow release is achieved and the action time of the tilmicosin is prolonged.
WO2014028669A1 Novel compounds for modulation of ror-gamma activity The present invention relates to aryl sulfones and related compounds that are modulators of ROR-gamma receptors. The invention also provides pharmaceutical compositions comprising these modulators, and methods of modulating ROR-gamma receptors using them. Also provided are methods of using aryl sulfones and related compounds as modulators of ROR-gamma to treat ROR-gamma mediated diseases.
US8318935 Organic compounds 75074 A compound of formula (I), or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M2, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5 and R5a are as defined herein for the for treatment of conditions treatable by the blockade of an epithelial sodium channel, particularly conditions benefiting from mucosal hydration.
US20080319073 Colonic delivery therapeutic agents for inflammatory bowel disease The present invention discloses a therapeutic agent for inflammatory bowel disease, which is in the from of delivering 1 to 5 g of glutamine to the large intestine per one administration; and the therapeutic agent for inflammatory bowel disease with which an anti-inflammatory agent(s) is combined. This therapeutic agent for inflammatory bowel disease can safely and effectively treat inflammatory bowel disease including ulcerative colitis without increasing the frequency of bowel movements.
CN101190937A Compound with liver-protecting activity The invention pertains to the technical field of medicine, relating to new compounds which have hepatoprotective activity or stereoisomer and salt thereof, the preparation methods of the compounds or the stereoisomer thereof, medical compositions which comprise the compounds or the stereoisomer and salt thereof as necessary active ingredients, and the application of the compounds or the stereoisomer and salt thereof in the preparation of medicine to cure and/or prevent hepatopathy and inflammatorydisease. The compounds or the stereoisomer and salt thereof of the invention have prominent functions of resisting acute and chronic hepatic injury and good function of antivirus at the same time, as well as prominent anti-inflammatory activity.
WO2011052706A1 Dry powder inhaler of tranilast having high solubility Provided is a dry powder inhaler of tranilast. Specifically disclosed are a dry powder inhaler comprising a solid dispersion, which is obtained by grinding tranilast crystals together with a dispersant and freeze-drying a suspension thereof, and an inhalation carrier, and so on. The aforesaid dry powder inhaler has an improved solubility and such properties as desired for an inhaler, i.e., a high uniformity and a high photostability. Moreover, the dry powder inhaler shows a high lung reaching proportion and, therefore, can exert an excellent effect even in a small dose.
DE102004004906A1 New oxygen-bridged angucyclinone derivatives, useful for treating bacterial infections and dementia, are modulators of intracellular calcium levels O-Bridged angucyclinones (I), their enantiomers, salts and solvates are new. - O-Bridged angucyclinones of formula (I), their enantiomers, salts and solvates are new.R1-R13 = hydrogen, 1-18C linear, branched or cyclic alkyl (optionally substituted one or more times), alkenyl, (hetero)aryl or benzyl (all optionally substituted one or more times), acyl (e.g. (trichloro)acetyl, formyl, fumaryl, maleyl, succinyl or benzoyl), branched chain or heteroatom- or aryl-substituted acyl, hydroxy, mercapto, alkoxy (e.g. 1-4C alkoxy where the alkyl is linear, branched or cyclic), alkylthio (e.g. (m)ethylthio), sulfonyl (e.g. SO3H, (trifluoro)methylsulfonyl, toluenesulfonyl or bromomethylphenylsulfonyl), or an N-bound substituent (e.g. amino (optionally substituted by 1 or 2 alkyl or aryl), cyano or nitro), fluoro, chloro, bromo, iodo, cyano or a heterosubstituent; or - (MK#2)CR1R2, CR4R5, CR6R7 or CR8R9 = C=O; and - (MK#3) R14-R16 = hydrogen, 1-18C linear, branched or cyclic alkyl (optionally substituted one or more times), alkenyl, (hetero)aryl or benzyl (all optionally substituted one or more times), acyl (e.g. (trichloro)acetyl, formyl, fumaryl, maleyl, succinyl or benzoyl), branched chain or heteroatom- or aryl-substituted acyl, hydroxy, mercapto, alkoxy (e.g. 1-4C alkoxy where the alkyl is linear, branched or cyclic), alkylthio (e.g. (m)ethylthio), sulfonyl (e.g. SO3H, (trifluoro)methylsulfonyl, toluenesulfonyl or bromomethylphenylsulfonyl). - Independent claims are also included for the following: - (1) method for producing (I) by culturing a Streptomyces; and - (2) method for synthesis of (I) by isolation or (partial) synthesis of the corresponding tetracyclic compound, epoxidation and cyclization by an epoxide-opening reaction. - ACTIVITY - Antibacterial; Neuroprotective. - MECHANISM OF ACTION - (I) sensitizes neurons, i.e. they are analogs of glutamate and induce release of calcium from intracellular stores. Neuronal cells were incubated with 3 mu g/ml gephyromycin (Ia: (I) with R3 = Me; R10 = hydroxy all other R groups = hydrogen), 0.2 mM glutamate and 2.5 mM calcium, resulting in a sharp increase in the concentration of intracellular calcium after 10 minutes, i.e. increasing the 340 nm/380 nm ratio for Fura-2-AM from 0.845 to 1.826. A similar effect was obtained in absence of glutamate or when the cells were incubated first with (Ia) and then with calcium.
CN101548968A Application of chroman compound HEF-19 in preparing intestinal canal smooth muscle antispastic and antidiarrhoeal The invention relates to the field medical technology, and discloses the applications of chroman compounds HEF-19 in preparing intestinal canal smooth muscle antispastic and antidiarrhoeal. In the in vitro experiment of animals, HEF-19 can reduce tension and amplitude induced by spontaneous activities of isolated small intestine smooth muscle of a rabbit, and relax the contractions induced by acetylcholine, barium chloride, potassium chloride and histamine on isolated small intestine smooth muscle of the rabbit. Therefore, the compound can be used for preparing antispastic and antidiarrhoeal for treating intestinal canal smooth muscle spasm. The applications of the compound refer to the preparations of medicaments used for treating stomach/abdomen convulsive pain caused by various reasons,medicaments used for treating intestinal irritable syndrome, medicaments used for treating functional disturbance gastrointestinal tract caused by ulcerative colitis, and medicaments used for treating functional diarrhea caused by various reasons and the like.
US20100120752 Muscarinic agonists to treat impulse control disorders The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are muscarinic, for example muscarine-1 (M1) agonists. These compounds are useful for the preparation of medicaments for treatment, amelioration or prevention of impulse control disorders. These include impulse control disorders ‘Not Elsewhere Classified,’ such as intermittent explosive disorder, pyromania, kleptomania, pathological gambling and trichotillomania, and impulse control disorders ‘Not Otherwise Specified,’ such as compulsive buying disorder, binge eating and binge drinking disorder, impulsive self-injurious behavior, sexual addictions, compulsive Internet use, and excessive mobile phone use.
CN101875601A Cresol trimer compounds as well as preparation method and application thereof The invention relates to cresol trimer compounds as well as a preparation method and application thereof. The compounds with novel structure are prepared from Penicillium expansum 091006 separated from a root sample of Excoecaria agallocha which is a mangrove plant. Proved by experiments, the compounds can be used as a cell proliferation inhibitor or antitumor agent.
US7608281 Retinoic acid receptors (RAR); tissue engineering, cartilage formation; for treatment of cartilage degenerative disease, skeletal trauma; bone morphogenetic protein (BMP), osteogenic protein (OP) The invention provides compositions comprising a RAR antagonist for promoting chondrogenesis and to methods employing such compositions for treating cartilage and associated bone abnormalities resulting from injury or disease and for ex vivo tissue engineering.
US7622484 Such as asthma or chronic obstructive pulmonary disease; a corticoid such as mometasone furoate and 5-(1-hydroxy-2-((5,6-diethylindan-2-yl)amino)ethyl)8-hydroxy-1,2-dihydroquinolin-2-one or salt such as maleate A medicament comprising, separately or together, (A) a compound of formula (I) in free or pharmaceutically acceptable salt or solvate form and (B) a corticosteroid, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease, the molar ratio of (A) to (B) being from 100:1 to 1:300.
US20080188466 Antiviral agent especially to treat hepatitis C virus infections; 5-Hydroxy-4-(7-methoxy-1,1-dioxo-1,2-dihydro-1 lambda 6-benzo[1,2,4]thiadiazin-3-yl)-2-(3-methyl-butyl)-6-thiophen-2-yl-2H-py-ridazin-3-one; side effects reduction The invention is directed to pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
WO2006129587A1 Pharmaceutical composition comprising pyrazolone derivative A pharmaceutical composition comprising a compound represented by the general formula (I) or a pharmaceutically acceptable prodrug or salt of the compound or a hydrate or solvate of the compound, prodrug or salt as an active ingredient. (I) wherein R1, R2, R3 and R4 are as defined in the description.
CN102144985A Potassium chloride elementary osmotic pump controlled release tablet and preparation method thereof The invention belongs to the field of medical technologies, in particular to a prescription and a process of a potassium chloride controlled release tablet. The process comprises the following steps of: by adopting ethyl cellulose, polyvinylpyrrolidone, hypromellose and the like as release blockers, adding an inert excipient, a lubricant and a coloring agent which are pharmaceutical acceptable according to a certain proportion to prepare a core tablet by using a suitable process; then, compounding cellulose acetate with a suitable coating additive to prepare a semipermeable membrane encapsulating the core tablet, and generating a drug release passage on the membrane to form a controlled release system of an elementary osmotic pump type for providing the zero-level release of potassium chloride.
CN101991693A Preparation method of medicament for treating tinea pedis The invention relates to a preparation method of a medicament for treating tinea pedis, which comprises the following steps of: firstly, decocting Szechwan pepper, white garden balsam, chaulmoogratree seeds, golden cypress, gallnut, belvedere fruits and Sophora flavescens in water, concentrating into a cream, grinding together with boric acid, salicylic acid, benzoic acid, table salt, alum and the like into fine powder, and subpackaging the fine powder. One package is used for each time and is soaked in warm water.
CN102755373A Medicine used for treating dermatophytosis The invention discloses a medicine used for treating dermatophytosis. The medicine is prepared by pigeonpea and rice vinegar; pigeonpea fruit, culm, leaf or root are cooked in water, and a certain amount of rice vinegar is added so as to prepare pigeonpea rice vinegar solution. In use, the pigeonpea rice vinegar solution and tepefaction water of 30-40 DEG C are adopted for preparing a foot bath solution according to the weight ratio of 1:100, and the time for foot bath is about 30-40 minutes each time. According to the clinic practical application, the treatment effect is notable, the medicine can be used for fundamentally curing dermatophytosis patients within 20-50 years old after being used for once, and can be used for fundamentally curing dermatophytosis patients within 50-70 years old after being used for twice.
CA2239072C Recombinant live vaccine containing feline herpes virus type 1, particularly for treating feline infectious peritonitis A recombinant live vaccine including, as the vector, a feline herpes virus that includes and expresses at least one nucleotide sequence coding for a polypeptide, said sequence being inserted in sites ORF5 and/or ORF2, is disclosed. A multivalent vaccine formula and feline herpes virus DNA fragments are also disclosed.
US20090214675 4-Chromenonyl-1,4-dihydropyridinecarbonitriles and the use thereof The present application relates to novel 4-chromenonyl-1,4-dihydropyridinecarbonitriles, processes for their preparation, pharmaceutical compositions containing them, and their use for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
WO2008073670A2 Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor Unit doses of factor Xa inhibitor compounds and methods of using these compounds for inhibiting blood coagulation in a human patient are taught herein. The unit dose of the factor Xa inhibitor compounds disclosed herein required to inhibit coagulation in a primate is lower than the unit dose required to obtain similar levels of coagulation inhibition in other animal models, such as rodents. Also taught are in vitro assays useful in predicting in vivo antithrombotic activity in humans.
CN102757426A Benzoisooxazolyl substituted thiazole compound, preparation method and application thereof The invention relates to a benzoisooxazolyl substituted thiazole compound represented by a formula (I), or pharmaceutically acceptable salts, solvates, prodrugs and isomers thereof. The invention further relates to a preparation method of the benzoisooxazolyl substituted thiazole compound, application of the benzoisooxazolyl substituted thiazole compound to preparation of antibacterial medicines, and pharmaceutical composition containing the benzoisooxazolyl substituted thiazole compound as an active component. The benzoisooxazolyl substituted thiazole compound is novel in structure, simple and convenient in synthesis method and good in antibacterial activity, and is applicable for the preparation of novel antibacterial medicines.
US20120135925 Covalent Inhibition of Bacterial Quorum Sensing Inhibitors of bacterial communication, such as quorum sensing, and method of use and manufacture thereof.
US20100267733 Synergistic Modulation of Microglial Activation by Nicotine and THC Treatment of microglial cells with nicotine and THC synergistically attenuate the microglial activation. Using microglial activation, the combination of THC and nicotine interact synergistically reduced LPS induced TNF-α release, showing that the combination of THC and nicotine clinically have greater efficacy in reducing neuroinflammation with less side effects than either drug given alone. CD40 signaling was found critically involved in pathological activation of microglial cells. This invention is also relevant to peripheral inflammation as well thru macrophages. In addition, other cannabinoids and other nicotinic-like medications currently in development are also covered under this discovery.
CN103202843A Application of pyrimidine derivative in preparation of drugs capable of prevention and/or treatment and/or adjuvant therapy of cancers The invention discloses application of a pyrimidine derivative in preparation of drugs capable of prevention and/or treatment and/or adjuvant therapy of cancers. The pyrimidine derivative comprises a pyrimidine compound having a structural formula (I), a pharmaceutically acceptable salt thereof, a solvate, a polymorphic substance, a tautomer and a prodrug or a composition containing the pyrimidine compound. The structural formula (I) is described in the specification. According to the invention, the pyrimidine derivative with novel Aurora kinase inhibition activity is formed through different C-N couplings and introduction of different pharmacophores respectively at positions 2, 4 and 6 of a pyrimidine ring, and the pyrimidine derivative can be used for preparation of drugs capable of prevention and/or treatment and/or adjuvant therapy of cancers.
US7022698 Pharmaceutical compositions containing new polymorphic forms of olanzapine and uses thereof Pharmaceutical compositions containing Form III, Form IV, Form V olanzapine and/or pharmaceutically acceptable salts thereof. The pharmaceutical compositions are useful for the treatment of psychotic conditions, mild anxiety and gastrointestinal conditions. In particular, the compositions are useful for treating schizophrenia and related disorders, acute mania, Bipolar I Disorder, psychotic mood disorder and psychosis in patients with Alzheimer's disease.
CN102775429A Preparation and application of unsaturation demethylation cantharides acid silver polymer The invention relates to a synthetic method and an application of unsaturation demethylation cantharides acid silver polymer. The material is colorless block crystal, the molecular formula is {[Ag(C8H7O5)].H2O}n, the n is degree of polymerization, and quantity of crystallization water is variable. The chemical name is poly-[[[mu3-(5,6-eta):kappaO2:kappaO2-(+-)-(1S,2S,3R,4R)-3-carboxyl-7-oxygen generation bicyclic-[2.2.1] heptane-5-alkene-2-carboxy anion] silver(I)-hydras], the structure is shown in the description: (the quantity of the crystallization water is variable). The polymer is simple in preparation method, good in purity and high in yield, has high toxicity on lung cancer cells (equal to cis-platinum), can restrain cancer cell proliferation, and is expected to be a highly-efficient and harmfulless antineoplastic drug.
US20120039800 Platinum Acridine Anti-Cancer Compounds And Methods Thereof Acridine containing cisplatin compounds are disclosed that show greater efficacy against cancer than other cisplatin compounds.
US20060040970 Administering 4,5 alpha -epoxy-6 beta -(3,4-dihydro-2H-benzo[1,4]thiazino)-3-methoxy-17-methyl-morphinan; for urinary frequency, therapeutic or prophylactic effect and of which side effects are improved The invention provides a morphinan derivative of the Formula (I): (wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(═O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like) or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.
US20120101141 Gel compositions and methods of use Improved topical gel compositions for the treatment of skin disorders are described. The gel compositions contain carbomer and methylparaben, and are substantially free of methylparaben crystalline particles after an extended period of storage.
WO2010106187A2 Inhibitors of cathepsin s for prevention or treatment of obesity-associated disorders The present invention relates to methods (and pharmaceutical compositions) for treating and/or preventing for obesity associated disorders, particularly related to a deregulation of glucose homeostasis, by administrating Cathepsin S inhibitors. The invention also relates to methods for diagnosing insulin resistance and glucose tolerance by measuring Cathepsin S levels in a biological sample obtained from a subject.
EP1950226A2 Receptors for human interleukin-12 The present invention is directed to IL-12 receptor proteins comprising a complex of the beta1 receptor protein with the beta2 receptor protein, which complex is capable of binding to human IL-12 with high affinity. When expressed in host cells the nucleic acid gives rise to substantially homogeneous IL-12 receptor proteins. Further, the invention relates to antibodies capable of binding to cells expressing the IL-12 receptor molecules.
US20080200555 Use of norepinephrine reuptake inhibitors for the treatment of tic disorders Selective norepinephrine reuptake inhibitors are used to treat tic disorders.
WO2007005670A3 Natural and synthetic sulfoxide, selenone and selenoxide analogs and polymer conjugated forms thereof for the modulation of angiogenesis The present invention relates to inhibiting angiogenesis with sulfoxide containing compounds, and polymeric forms thereof, in mammals including animals and humans. Sulfoxide containing compounds, and polymeric forms thereof , can be used alone or in combination with standard therapies to inhibit angiogenesis-mediated disorders. The present invention also relates to the combined use of sulfoxide containing compounds, and polymeric forms thereof , with other anti-angiogenesis agents, with various anti- inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer, and with laser, photodynamic therapy for ocular-related disorders such as diabetic retinopathy or age-related macular degeneration.
CN101879190A Composition containing curcumin and application of curcumin in preparing composition for adjusting blood sugar The invention discloses a composition containing curcumin and application of curcumin in preparing a composition for adjusting blood sugar, relating to a composition and application thereof. The invention solves the problems that the traditional drugs for treating diabetes mellitus has long taking period and easily cause toxic or side effect. The composition containing curcumin contains trivalent chromium and curcumin and is used for adjusting blood sugar. The composition containing curcumin can achieve blood sugar reduction effect after being taken for 7 weeks when used for treating diabetes mellitus and can effectively control the rise of blood sugar after treatment for 7 weeks, has short treating period and no toxic or side effect when used for treating diabetes mellitus.
US7368565 Methods for preparation of cytotoxic conjugates of maytansinoids and cell binding agents The present invention discloses a one-step process for the production of cytotoxic conjugates of maytansinoids and cell binding agents. Maytansinoids having a disulfide linker that bears a reactive moiety are linked to cell binding agents, such as antibodies, without prior modification of the cell binding agent. These conjugates are useful as therapeutic agents which are delivered specifically to target cells and are cytotoxic.
CA2334119C Pharmaceutical composition with tumor necrosis factor a and 2-methoxyestrone-3-o-sulphamate for inhibition of estrone sulphatase A composition is described. The composition comprises i) a compound comprising a sulphamate group ("a sulphamate compound"); and ii) a biological response modifier.
EP2135867A1 Trans-9, 10-dehydroepothilone C and trans-9, 10-dehydroepothilone D, analogs thereof and methods of making the same The present invention provides new trans-9,10-dehydroepothilone C and trans-9,10-dehydroepothilone D based derivative compounds, compositions and methods of inhibiting cellular hyperproliferation and/or stabilizing microtubules in vitro and of treatment of hyperproliferative diseases in vivo. Also disclosed are methods of making the compounds.
US20090143433 Cocktail for modulation of alzheimer's disease Formulations for the prevention and treatment of neurological diseases and cognitive deficiencies, i.e., Alzheimer's Disease (AD), Parkinson's Disease, amyotrophic lateral sclerosis, mild cognitive impairment and other types of dementia, comprise therapeutically effective amounts of curcumin, piperine, epigallocatechin-3-gallate (EGCG) and n-acetylcysteine. The combination addresses some or all of the pathways which can result in neurological deficiencies, degeneration and diseases.
EP1789057B1 Neuroprotective effect of solubilized udca in focal ischemic model The present disclosure provides compositions and methods for treating, ameliorating, or relieving at least one symptom associated with loss of blood flow to the brain including, without limitation, ischemic stroke. Compositions of the disclosure may comprise a bile acid compound and a carbohydrate, wherein both materials remain in solution for all pH values of the solution within a selected range of pH values. Symptoms may include infarct volume, functional recovery, apoptosis, and/or eNOS expression.
WO2012151452A1 Pyruvate kinase activators for use in therapy Described herein are methods for using compounds that activate pyruvate kinase.
CN103083370A Novel application of total flavones of hippophae rhamnoides The invention provides application of total flavones of hippophae rhamnoides in preparation of treating diabetic retinopathy. The invention also provides a medicine composition for treating the diabetic retinopathy. The medicinal flavonoid compound can be used for resisting the oxidative damage of hydrogen peroxide, improving the activity of cells as well as the oxidation reduction function, and bringing protection to the retinal pigment epithelium (RPE), so that photoreceptor cells can be protected, the macular oedema is reduced, the vision is improved, and the total flavones of hippophae rhamnoides are expected to be developed into a new medicine for treating the diabetic retinopathy.
US20120225939 Use of Prostaglandins F2Alpha and Analogues for the Healing of Corneal and Conjunctival Lesions The invention relates to a composition for use in treating corneal and conjunctival lesions, wherein the composition comprises a prostaglandin F2alpha or analogue, in a therapeutic amount, said composition being in a form suitable for topical application on the ocular surface and is free of deleterious preservative; the invention also relates to a method for treating surface ocular conditions in a patient in need thereof, comprising administering a composition of the invention.
CN101214285A Use of giant knotweed rhizome extract in preparing product for resisting AIDS virus and hepatitis B The present invention relates to purposes of giant knotweed extract. The in vitro anti-HIV experiment shows that resveratrol 3-O-Beta-D- glucoside 2íÕ-sulfate sodium or potash salt and resveratrol 3-O-Beta-D- glucoside 4íÕ-sulfate sodium or potash salt show significant activity of resisting hepatitis B virus; resveratrol 3-O-Beta-D- glucoside 2íÕ-sulfate sodium or potash salt also has significant HIV inhibited effect. The virus infectious diseases such as AIDS and hepatitis B poses a serious threat to human's health and life and hepatitis B is one of the major diseases affecting human's health. The present invention provides a lead compound for doing R&D of novel anti-HIV and hepatitis B virus medicines and also a novel medicine source for clinic application, thus having a significant value to develop and utilize the medical plant resources of our country.
CA2805075A1 Composition comprising retinol, a precursor or a reaction product of it and a plant extract from at least one chamomilla plant for the treatment of cancer The invention relates to a (i) Vitamin A, a reaction product, a metabolite or a precursor of it and (ii) a plant extract of chamomile or an active component thereof, preferably for use in the treatment of cancer. The inventive composition may be provided as a medicament or a pharmaceutical composition. The at least one Chamomilla plant typically contained in the inventive compositions preferably comprises Matricaria recutita, more preferably flores tubiformis of Matricaria recutita. Esters of Retinol typically contained in the inventive compositions typically comprise e.g. Retinyl acetate and a plant extract from the plant Matricaria recutita.
WO2010070117A1 Treatment method by the administration of anti-her2 targeted active compounds to patients with early breast cancer and her2-negative primary tumor The present invention is related to an anti-HER2 therapeutic active compound for use in the treatment of breast or bladder cancer in patients having HER2-negative primary breast or bladder cancer and biomarkers predictive for response to anti-HER2 targeted therapeutic active compounds, including but not limiting to HER2+ CTCs.
US20080076727 antibody cocktails each recognizing a distinct epitope on the HMW-MAA protein; HMW-MAA antibody cocktails and their uses in detecting cancer and isolating cancer cells are disclosed. Also disclosed are methods of detecting cancer based on the presence of an HMW-MAA genomic sequence in circulating DNA, as well as the increased expression of the HMW-MAA gene and the reduced methylation of the HMW-MAA gene promoter in tissues and circulating cells.
US20100166780 CpG Oligonucleotide Analogs Containing Hydrophobic T Analogs with Enhanced Immunostimulatory Activity The invention relates to oligonucleotides including at least one lipophilic substituted nucleotide analog and a pyrimidine-purine dinucleotide. The invention also relates to pharmaceutical compositions and methods of use thereof.
US20110092591 Phenyl-prenyl derivatives, of marine and synthetic origin, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders The present invention is related to a family of phenyl-prenyl derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or Parkinson's Disease. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the compounds of formula (I) for medical use, particularly for the use for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder, and to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder.
EP1718292A1 Furosemide derivatives as modulators of hm74 and their use for the treatment of inflammation disorders Furosemide-like molecules with agonist activity on the HM74 receptor having the following structure formula (I); and their use to treat inflammatory disorders.
US7067553 Thiourea compounds and the pharmaceutical compositions containing the same The present invention relates to thiourea compounds and the pharmaceutical compositions containing the same, and particularly, to novel thiourea compounds as an antagonist against vanilloid receptor (VR) and the pharmaceutical compositions thereof. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.
CN1634905A Use of Lignans compound used for anti-osteoporosis medicine The invention relates to the use of lignans compound used for anti-osteoporosis medicine. The stem and branch of elderberry are heated and refluxed by alcohol and extracted to obtain alcohol extractive, alcohol extractive is mixed and suspended in water and extracted by chloroform, ethyl acetate, and n-butyl alcohol, chloroform extract and ethyl acetate extract are separated by chemical method to obtain lignans compounds carolignan L, carolignanM, and buddlenol G for treating osteoporosis.
CN1883458A Enteric coated preparation of lansoprazole sodium and preparation method thereof Disclosed is a Lansoprazole sodium intestine-dissolving preparation, which is prepared from Lansoprazole sodium 15-30 parts, thinning agent 150-300 parts, moistening agent or binding agent 20-110 parts, crumbling agent 5-25 parts, lubricating agent 5-15 parts and coating agent 30-100 parts through the steps of disintegrating, sieving, mixing, tabletting, and dressing isolation layer.
CA2553221A1 Folate conjugates and complexes Disclosed are conjugates and complexes that include a folate receptor ligand and one or more therapeutic molecules, such as onconase or a variant thereof such as rapLR1. The conjugates and complexes may be useful as primary therapeutic agents, which may be administered with additional therapeutic or diagnostic agents. Also disclosed are kits that include the conjugates and complexes.
CN101342155B (R,R)-formoterol inhalation dust cloud agent and preparation method thereof The invention discloses (R,R)-formoterol powder inhalation which is composed of carrier powders and (R,R)-formoterol medicine carrier powders; wherein, the content of the medicine carrier powders is 5 percent to 80 percent (w/w), and the particulate diameter of at least 90 percent (w/w) of powder particulate is smaller than 10Mum; the content of the carrier powders is 20 percent to 95 percent (w/w), and the particulate diameter of at least 80 percent (w/w) of powder particulate is smaller than 40Mum to 100Mum. The powder inhalation of the invention is prepared by the follower steps: 1) preparing the carrier powders with a solvent crystallization method; 2) preparing the medicine carrier powders with a spray drying method; 3) mixing the medicine carrier powders and the carrier powders to obtain the preparation. The power inhalation of the invention has favorable fluidity and lower moisture-absorptivity; the preparation method is easy to operate, the cost is low, and the invention solves the problem of great disparity between main drug and auxiliary material.
WO2006121389A1 Use of a neurokinin-2 receptor antagonist for treating or preventing detrusor overactivity Treatment of detrusor overactivity in a subject comprising the administering a therapeutically-effective amount of a neurokinin-2 receptor antagonist or pharmaceutically-acceptable salt thereof and pharmaceutical compositions containing such a compound.
US7560425 Pharmaceutical composition consisting of rapamycine and gastrin 17(LEU15) and a method for treating diabetes Compositions and methods for islet neogenesis therapy comprising an EGF and a gastrin in combination with immune suppression, and for treating or preventing early stage diabetes with a gastrin/CCK receptor ligand and an immunosuppressant are provided.
CN103565765A Preparation of ibuprofen orally-disintegrating pellet coated by compound essence powder and capable of hierarchically releasing drug The invention relates to an ibuprofen orally-disintegrating pellet coated by compound essence powder and capable of hierarchically releasing drug. The pellet can cover the spicy taste in the mouth and hierarchically release drug. The preparation method of the ibuprofen orally-disintegrating pellet comprises the following steps: pulverizing ibuprofen micro-particles until the particle size is less than 200 [mu]m; then carrying out three coating processes with three kinds of powder: (1) drug releasing in the mouth: coating part of ibuprofen with compound essence powder so as to obtain orally-disintegrating pellets (I); (2) drug releasing in the stomach: coating part of ibuprofen with gastric soluble powder so as to obtain orally-disintegrating pellets (II); (3) drug releasing in the intestine: coating part of ibuprofen with enteric powder so as to obtain orally-disintegrating pellets (III); evenly mixing the orally-disintegrating pellets (I), (II) and (III) with a vertical press filling agent, a compound disintegrating agent, a flow aid, a lubricant, and a taste modifying agent, and then pressing the mixture into tablets. In the preparation method three orally-disintegrating pellets are prepared, besides the spicy taste of ibuprofen in the mouth is covered, hierarchical releasing of drug in the mouth, stomach, and intestine is achieved, and no prominent grit feeling exists.
CN101366761A Pharmaceutical combination for preventing birth defect and improving anamnesis The invention relates to a medical composition for preventing birth defects and improving memory, which comprises Langehead Atractylodes Rhizome, sea backthern, vitamin A, beta carotene, vitamin B complex, vitamin C, vitamin D, vitamin E, and macroelements of calcium and magnesium. The medical composition is mainly suitable for pregestational women, pregnant women and wet nurses, is very effective in preventing the birth defects and improving the memory, has both health care and tonic efficacies, and does not generate any side effects even after long-term application.
CN101342165A Instant gel rubber of thyroxine liothyronine for eyes The invention discloses immediate type ophthalmic gelatin of thyroxine liothyronine and a preparation method thereof. 100 milliliters of the immediate type ophthalmic gelatin of thyroxine liothyronine contains 0.1 to 3 grams of thyroxine powder extract, 0.05 to 1 grams of preservative, 1.0 to 7.5 grams of permeation pressure conditioning agent and 30 to 150 grams of gelatin substrate. Remaining components are acid-base buffer regent and water for rejection. The invention enriches the dosage forms of the thyroxine powder extract by optimizing auxiliary materials and improving technology so that lag time in eyes is greatly prolonged and curative effect is improved without adverse stimulus reaction.
US7304060 Enzyme inhibitors for antidiabetic agents, antitumor disorders, treatment of skin disorters, anticancer agents and cognitive activators for Alzheimers disease treatment The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
US7238684 Benzothiadiazepine derivatives, processes for their preparation and pharmaceutical compositions containing them The present invention relates to compounds of formula (I): wherein Rv, R1, R2, Rx, Ry, R3, R4, R5, R6, Rz and v are as defined within; pharmaceutically acceptable salts, solvates, solvates or such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.
EP0690724B1 Chlamydia vaccine comrising anti-idiotypic antibodies A genus specific chlamydia vaccine is provided which comprises an anti-idiotype antibody capable of producing in an animal an anti-anti-idiotypic antibody which recognizes a glycolipid exoantigen (GLXA) of chlamydia. The vaccine is produced by producing an idiotypic antibody to GLXA which, in turn, is utilized to produce the anti-idiotypic antibody comprising the vaccine.
EP2499137A1 Palonosetron metabolites Provided are metabolites of palonosetron that can be used in treating animals, particularly humans, of the formula (I): or a pharmaceutically acceptable salt or prodrug thereof; wherein R1 and R4 independently can be H, hydroxyl, or carbonyl; and wherein R3 can be Formule (II) or Formule (III).
CN101098861A Derivatives of isothiazol-3 (2h)-thione 1,1-dioxides as liver x receptor modulators The present invention relates to certain novel compounds of formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) a (NR1H3) and/or ss (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
CA2589638C 7-membered ring compound and method of production and pharmaceutical application thereof A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved:(see formula I) a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.
CN103570715A Salt of uncaria alkaloid derivative The invention relates to fumarate of uncaria alkaloid derivative, namely geissoschizine methyl ether, or a pharmaceutically acceptable solvate of the uncaria alkaloid derivative and application of the uncaria alkaloid derivative in preparation of an acetylcholin esterase inhibitor medicine.
CN101396333A Eye in-situ gel of chiral anti-glaucoma medicine L-3alpha alkyla acyloxy-6belta alkyla acyloxy tropane and preparation method thereof The invention relates to an ophthalmic in-situ jelly of chiral anti-glaucoma medicine levofloxacin tropane. The ophthalmic jellies concretely comprises 0.03 percent to 0.3 percent of levofloxacin tropane, 10 percent to 20 percent of hydrophilic polymer material, 0 percent to 20 percent of humectant, 0.1 percent to 10 percent of permeation pressure regulator, 0.01 percent to 0.3 percent of antiseptic/bacteriostat, pH value regulator and water. In a preparation method, the materials are weighted according to the percentage; the levofloxacin tropane is solved in injection water, the hydrophilic polymer material is added under the stirring state, and the solution is stood over a night; the adjuvant such as the humectant and the like is added, and the pH value is adjusted as 4 to 9; the solution is filtered, the injection water is added to the total quantity, and the ophthalmic in-situ jelly is obtained. The ophthalmic in-situ jelly has the advantages of uniform and smooth quality, proper viscosity, convenient use, exact dosage, and long-term uniform distribution on the surface of eye cornea; besides, the jelly causes no hypersusceptibility and irritation, no blurred vision, can effectively prolong the acting time of the medicine on the eye cornea, and has wide application prospect.
US20060002888 Polyionenes for treating infections associated with cystic fibrosis A method of using ionene polymers for the treatment or prevention of infections (e.g., pulmonary infections) in cystic fibrosis patients is provided. The method comprises administering to a mammal an effective amount of an ionene polymer to prophylactically or therapeutically treat infections associated with cystic fibrosis.
CN102670527A Freeze-dried powder injection of L-oxiracetam and process for preparing freeze-dried powder injection The invention relates to a freeze-dried powder injection of L-oxiracetam and a process for preparing the freeze-dried powder injection. The freeze-dried powder injection comprises, by weight, 1 part of the L-oxiracetam, 0.1 to 10 parts of an excipient, 0.01 to 1 part of an antisticking agent and 0.01 to 0.5 part of a pH regulator, wherein polyethylene glycol (PEG) series of products serve as the antisticking agent preferably. The freeze-dried powder injection which is prepared on the basis of a prescription according to the process has the advantages of being short in freeze-drying time, attractive in appearance, short in redissolving time and high in stability.
WO2013044736A1 Traditional chinese medicine composition for external use in treating xerophthalmia and the preparation method thereof Traditional Chinese medicine composition for external use in treating xerophthalmia and preparation method thereof, wherein the raw material of the traditional Chinese medicine composition consists of Radix Scutellariae, Herba Menthae, Radix Trichosanthis, Flos Chrysanthemi, Rhizoma Polygonati and Broneolum Syntheticum.
EP1209988B1 Cross-linked agent for generation of a long-lasting satiety effect and method for the production of the said The invention relates to an orally administered agent containing stable, uronic acid-containing polysaccharides cross-linked to each other and in the form of a sponge-like structure which dissolves poorly in water and/or gastrointestinal liquids or can be poorly resorbed. A method for the production and application of the said agent is also disclosed.
CN103664879A Compounds for treating traumatic brain injury diseases and application thereof The invention discloses compounds, and a pharmaceutical composition and new application thereof in preparing medicines for treating traumatic brain injury diseases. The compounds for treating traumatic brain injury diseases can have very obvious effect.
CN102008723A Compound preparation of diclofenac sodium and triptan medicines for treating migraine The invention discloses a compound preparation of diclofenac sodium and triptan medicines for treating migraine, prepared from diclofenac sodium or pharmaceutical salts thereof and any one triptan medicine or pharmaceutical salts thereof used as main ingredients and matched pharmaceutical vectors. The preparation contains 25-4150mg of diclofenac sodium and 1.0-150mg of triptan medicaments. The invention has the advantages of fully exerting the pharmaceutical complementary synergism according to medicament combination, lessening the adverse reaction related to a certain increased dosage and effectively treating migraine. The compound preparation of the invention has the advantages of short course of treatment, rapid effect, less side effect and low cost.
CN1858052A Quinolone carboxylate compounds and their preparing method and use The present invention discloses a kind of quinolone carboxylate compounds and their preparation process and pharmaceutically acceptable salts. Pharmacological tests show that these compounds have obvious bacteriostasis on both Gram-positive bacteria and Gram-negative bacteria.
EP2498778A1 Diazeniumdiolated compounds, pharmaceutical compositions, and method of treating cancer Disclosed is a method of treating cancer in a patient comprising administering to the patient an effective amount of a diazeniumdiolated (N2O2-containing) compound or a pharmaceutically acceptable salt thereof, wherein the cancer cell has an elevated level of reactive oxygen species (ROS) and/or a decreased level of one or more of PRX1, PRX6, and OGG1, compared to a normal cell of the same tissue or tissue type. An example of a diazeniumdiolated compound is Formula (I), wherein X and Q are defined herein. Also disclosed are diazeniumdiolated compounds, pharmaceutical compositions, and methods of use including enhancing the chemotherapeutic treatment of chemotherapeutic agents and high energy radiation.
US20110136905 Crystalline teglicar The present invention relates to a new crystalline form of R-4-trimethylammonium-3-(tetradecylcarbamoyl)-amino butyrate (also named crystalline Form I of ST 1326 or teglicar), a process for its preparation and pharmaceutical compositions containing same.
WO2010005528A2 Pyrrolopyridine carboxylic acid derivatives Disclosed are compounds and pharmaceutically acceptable salts of Formula (I) wherein R1, R2, R3, and RN are as defined herein. Compounds of Formula (I) are useful in the prevention and/or treatment of neurological and psychiatric disorder, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the disclosure and methods of treating the aforementioned conditions using such compounds.
EP2041143A1 Quinazoline derivatives, their preparation, their use as tyrosine kinase inhibitors and medicaments comprising them The present invention relates to a quinazoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).
CN102145016A Pharmaceutical composition containing vitamins and minerals The invention belongs to the field of medicines or health foods, in particular to a pharmaceutical composition containing vitamins and minerals. The pharmaceutical composition contains the following components in parts by weight: 1-10 parts of cordycepic acid and/or probiotics, 0.05-3 parts of vitamins and 0.05-3 parts of minerals. Proved by pharmaceutical tests, the pharmaceutical composition provided by the invention has the favorable function of improving immunizing power.
CN103006638A Application of aphanamixoid A in preparing medicament for treating hemorrhagic fever with renal syndrome The invention discloses an application of aphanamixoid A in preparing a medicament for treating hemorrhagic fever with renal syndrome. Researches of aphanamixoid A in virus in-vitro and in-vivo inhibition experiments of hemorrhagic fever with renal syndrome indicate that the aphanamixoid A has low toxicity to cells, can directly kill virus of hemorrhagic fever with renal syndrome, can remarkably inhibit multiplication of the virus, and can remarkably protect susliks infected by the virus, so that the attack time is postponed, the disease course is prolonged, and the death rate is reduced. Therefore, the aphanamixoid A is an effective and safe medicament for treating hemorrhagic fever with renal syndrome.
US20100256240 Prostacyclin derivatives This invention relates to novel prostacyclin derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors.
WO2012123563A1 Benz imidazole derivatives as inhibitors of glutaminyl cyclase The invention relates to novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
WO2008071398A1 Sulfonamides and their use as a medicament The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, -SO2R, wherein R is phenyl or morpholino, -NC(O)Me, -NC(O)Et, - CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, -COOMe, -COOEt, RC(O)N-, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2-, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, - MeOC(O)-, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting of -NH-NH-, -NH-NH-CH2-, ethinyl, -NH-C(O)-CH2-, - NH-NH-SO2-, -C(O)-NH-CH2-, -NH-N=CH-, -NH-N=C(Me)-, a -NH-N=CH- motif being part of a heterocyclic system, preferably a substituted or unsubstituted pyrazole or pyridazine system, and pharmaceutically active salts thereof. Further, the invention relates to the use of these compounds as a medicament, especially for the treatment of cancer.
EP1206466B1 Alkoxy substituted benzimidazole compounds, pharmaceutical preparations containing the same, and methods of using the same Compounds represented by formula (Ia) are disclosed by the invention, along with compositions and complexes thereof, optionally in combination with compounds of formula (Ib). Pharmaceutical formulations and methods of making and using such compounds are also disclosed.
US8053576 Treating conditions associated with the nociceptin/ORL1 receptor system, e.g. pain, drug withdrawal, anxiety, muscle relaxants, anxiolytic agents; e.g. 1,1-[3-dimethylamino-3-(pyridin-2-yl)pentamethylene]-3,4-dihydro-1H-2,9-diazafluorene Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.
WO2007118984A1 Use of (s)-roscovitine for manufacturing a medicine This invention relates to the use of 6- ( benzyl-amino ) -2 ( S) - [ 1 ( hydroxymethyl ) propyl ] amino ] - 9-isopropylpurine) or at least one of its pharmaceutically acceptable salts for manufacturing a medicine intended for prevention and/or treatment of neurological diseases, particularly associated with neurological lesions.
US20080221108 Anthranilic Acid Derivatives As Hm74A Receptor Agonists Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2 and W, are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
CN102366403A Colchicine microemulsion transdermal agent, preparation method thereof and application thereof The invention discloses a colchicine microemulsion transdermal agent, a preparation method thereof and an application thereof. The colchicine microemulsion transdermal agent comprises lecithin, n-propanol, a surfactant, colchicine and an assistant. The colchicine microemulsion transdermal agent of the invention can be used for the preparation of drugs for treating gout. A microemulsion system of the colchicine microemulsion transdermal agent of the invention can promote colchicine to effectively permeate skins, so a purpose of gout treatment is reached, and toxic side effects of oral administration to livers and kidneys of human bodies are simultaneously reduced.
CN101416979A Use of oligosaccharide in preparing medicine for treating tumor and inhibiting tumor metastasis The invention relates to the biological medicine, in particular to the application of chitosan oligosaccharide in preparing medicines used for treating tumors and restraining tumor metastasis, wherein, by taking a nutrient solution for tumor cells as an inducing factor and taking a human umbilical vein endothelial cell as an study object, the chitosan oligosaccharide can significantly restrain the human umbilical vein endothelial cell metastasis induced by the nutrient solution for tumor cells and the formation of tubular structure caused by the endothelial cell metastasis, but have no obvious restraining effect on the proliferation of the human umbilical vein endothelial cells metastasis induced by the nutrient solution for tumor cells.
US7638540 Benzofuran compound and medicinal composition containing the same The present invention relates to a benzofuran compound of the formula (I) wherein each symbol is as defined in the description, a pharmaceutically acceptable salt thereof and the like. The compound of the present invention has superior leukotriene inhibitory action, BLT2 competitive inhibitory action, BLT2 blocking action, action for the prophylaxis or treatment of allergy, action for the prophylaxis or treatment of asthma and action for the prophylaxis or treatment of inflammation, and is useful as an agent for the prophylaxis or treatment of diseases such as allergic disease, asthma, inflammation and the like, and other diseases.
EP2047844A2 A method of microencapsulation A method for microencapsulation of substances is provided. The substance(s) is/are dissolved or dispersed in an organic solvent of the kind that is partially miscible in water media. This organic solution is then mixed with an aqueous solution, which is saturated with an organic solvent and an emulsifier to form an emulsion. The emulsion is then poured into water under continuous agitation for the extraction of residual solvent. The formation of the solid capsules takes place during this extraction process. The capsules are undergone to further purification, whereby the microcapsules can be separated from the water and dried. By conditions of incubation of microcapsules in water-containing formulations the wall-softening process takes place. The unique system for controlled releasing the ingredients from microcapsules is based on the above-mentioned process.
CN101054356A Sodium acetylcysteine for removing phlegm and curing hepatopathy and preparation method thereof The present invention relates to a sodium acetylcysteine medicine for curing acute and chronic hepatopathy, which have above structural formula. The present invention also provides method for preparation of above sodium acetylcysteine, including performing acid-base salt reaction in general organic solvent by using acetylcysteine reacting with general inorganic base, which assisted by mercapto protecting agent and reaction system de-watering agent during the reaction process, adding precipitating agent to precipitate after reaction is finished, then preparing sodium acetylcysteine by filtrating and drying. The sodium acetylcysteine provided in present invention has advantages of high stability, low toxicity, exact curative effect and convenience in clinic application.
US20110034534 siRNA compounds and methods of use thereof The present invention relates to compounds, pharmaceutical compositions comprising same and methods of use thereof for the inhibition of certain genes, including SOX9, ASPP1, CTSD, CAPNS1, FAS and FAS ligand. The compounds and compositions are useful in the treatment of subjects suffering from diseases or conditions and or symptoms associated with diseases or conditions in which gene expression has adverse consequences.
US8034818 Therapeutic uses of derivatives of piperidinyl- and piperazinyl-alkyl carbamates Therapeutic uses of a compound corresponding to the general formula (I): in which A=N or CR2; R2=H, F, OH, CN, CF3, C1-6-alkyl, C1-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3=CHR4CONHR5; R4=H or C1-6-alkyl; R5=H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate.
WO2013147556A1 Pharmaceutical composition for preventing or treating hearing loss, containing cilostazol and ginkgo leaf extract as active ingredients The present invention relates to a pharmaceutical composition for preventing or treating hearing loss, containing cilostazol and a ginkgo leaf extract as active ingredients. The pharmaceutical composition can effectively prevent or treat noise-induced hearing loss or ototoxic hearing loss by inhibiting the apoptosis of hair cells due to the generation of reactive oxygen species (ROS).
WO2013041238A1 Use of kibra peptides, hdac inhibitor or proteasome inhibitor for improving anxiety disorders The invention, among others relates to a peptide comprising the sequence FVRNSLERRSVRM, said peptide having a sequence selected from the group consisting of SEQ ID NOs 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42 - or having a sequence a sequence of 13 to 40 consecutive amino acids of SEQ ID NO: 42 or of a peptide derivative thereof or of a peptide conjugate of the peptide or the peptide derivative for use in a method for treating anxiety disorders.
WO2010044441A1 Acetic acid amide derivative having inhibitory activity on vascular endothelial lipase Disclosed is a compound useful as a vascular endothelial lipase inhibitor. Specifically disclosed is a pharmaceutical composition having an inhibitory activity on vascular endothelial lipase, which comprises a compound represented by formula (I), a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt. The substituents contained in formula (I) are as defined in the description of the present application.
US20110243938 Methods to Reduce B-Helper T Cells to Treat Autoimmune Diseases The present invention includes compositions and methods for the treatment of autoimmune diseases by administering to a subject having an autoimmune disorder an effective amount of a therapeutic composition comprising a pharmaceutically acceptable carrier and at least one IL-12 inhibitor, e.g., a blocking anti-IL-12 antibody or fragment thereof.
CN102068453B Stable complex vitamin composition and preparation method thereof The invention relates to an aqueous solution for preparing a stable complex vitamin composite, a complex vitamin composite injection and a preparation method thereof. The composite is prepared from 11 vitamins, or analogs thereof, racemization alpha-tocopherol, polysorbate and medically acceptable auxiliary materials by the freeze drying technology, wherein 11 vitamins comprises vitamin A palmitate, vitamin D3, vitamin C, cocarboxylase tetrahydrate, riboflavin sodium phosphate, vitamin B6, vitamin B12, folic acid, dexpanthenol, biotin and nicotinamide. Compared with the prior art, the composite has better stability.
CN1903312A Extractive of bulb of Anhui fritillary, prepn. method and use thereof An extract of Anhui tendrilled fritillary bulb and its preparing process are disclosed. It can be used to prepare the medicines for treating cough and asthma and resolving phlegm.
CN101023952A Use of aesin in releasing abdominal distention and astriction The present invention provides a new application of aescine. The invented tests show that the invented aescine can be mainly used for curing the diseases of abdominal distension and constipation, etc, due to gastrointestinal peristalsis reduction and gastrointestinal dysfunction resulated from diabetes, angiocardiopathy, senile diseases and other diseases. It can obtain obvious therapeutic effect for curing abdominal distension and constipation, etc.
CN102307862A Compounds for treating cancer Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.
US6949263 Method for preparing nicotianamine or nicotianamine-containing product Precipitation fractionation of an aqueous extract of soybeans by addition of an organic solvent such as ethanol or molecular weight fractionation of the extract by ultrafiltration or size exclusion chromatography is appropriately combined with activated carbon filtration, cation- or anion-exchange resin treatment or other adsorbent (e.g., polyamide or octadecylsilica) treatment to provide a nicotianamine product of desired purity. The product is added to food and drink to provide health foods.
CN101254180B Nimodipine capsule containing semi-solid combination and preparation The invention discloses a nimodipine capsule with high dissolution and semi-solid composition as content and a preparation method thereof, and belongs to the pharmaceutical preparation field. The method comprises the following steps of mixing micronized nimodipine and a hydrophilic carrier, preparing into solid dispersion by melting extrusion method, cooling, pulverizing, mixing with semi-solid matrix, surfactant, melting point regulator under heating, and filling the content into hard capsule with a capsule filling machine. The invention combines the melting extrusion technique and semi-solid filling hard capsule technique, and after the prepared novel nimodipine capsule is administered into human body, the nimodipine quickly diffuses in molecular form and saturates metabolic enzymes, soas to improve bioavailability. The inventive nimodipine capsule solves the low dissolution and low utilization ratio problems of prior nimodipine preparation; and has the advantages of high dissolution, good stability, simple preparation method, and applicability to industrial production.
EP1219630B1 Immunopotentiating compositions Immunopotentiating compositions containing lactose/fructose oligosaccharides as the active ingredient and compositions accelerating the production of interferon-η, in particular, in the form of foods. Administration or intake of these compositions can potentiate the biological protective mechanisms (immune functions) in the digestive tract and thus achieve remarkable effects of preventing and treating digestive infective diseases, etc.
US20100278878 Quetiapine salts and their polymorphs The present invention relates to novel and stable salt forms of quetiapine, processes for preparation, pharmaceutical compositions, and method of treating thereof. More particularly, the present invention provides novel acid addition salts of quetiapine wherein the acid counter ion is provided by an acid selected from the group consisting of benzene sulfonic acid, dibenzoyl-L-(+)-tartaric acid and di-p-toluoyl-L-(+)-tartaric acid. The present invention also provides novel polymorphic forms of quetiapine salts selected from the group consisting of quetiapine hydrobromide, quetiapine sulfate, quetiapine nitrate and quetiapine citrate.
US20080226722 Gel Composition Comprising Charged Polymers Aqueous gel compositions are disclosed which are useful as drug carriers for controlled delivery applications, such as for parenteral depot formulations. The gels comprise ionically charged microparticles, and preferably mixtures of oppositely charged microparticles. The microparticles can be loaded with active compounds, such as therapeutic peptides and proteins. The gels can be prepared by combining oppositely charged microparticles in the presence of water.
US20050153967 Pharmaceutical compositions comprising 2-(4-ethoxy-phenyl)-3-(4-methanesulfonyl-phenyl)-pyrazolo'1,5-bipyridazine in nanoparticulate form The invention provides a pharmaceutical composition comprising a compound of formula (I) and pharmaceutically acceptable salts thereof, in which the compound is present in solid particles in nanoparticulate form, in admixture with one or more pharmaceutically acceptable carriers or excipients.
EP1922303A2 Purification of paricalcitol The present invention is directed to a novel process for preparing Paricalcitol wherein Paricalcitol, dissolved in a solvent, is precipitated from a concentrated or seeded solution.
EP1525199A1 Substituted thienyl-hydroxamic acids as histone deacetylase inhibitors A compound of formula (I): which can be used in the treatment of diseases associated with histone deacetylase enzymatic activity.
US8022077 Pyrido[2,3-d]pyrimidines useful as HCV inhibitors, and methods for the preparation thereof The present invention relates to the use of pyrido[2,3-d]pyrimidines of formula (I) wherein L, R1, R2 and R3 have specific meaning. The present invention also relates to the use of the compounds of formula (I) as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds of formula (I) per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.
WO2013061279A4 Uses of indole-ketones or indolidones as neuro-protective drugs The present invention provides a method of using indole-ketone or mdolidone to treat or prevent a neurodegenerative disease or disorder. In one embodiment, the neurodegenerative disease is Parkinson's disease. In another embodiment, the neurodegenerative disease or disorder is associated with excessive neuronal Nitric Oxide Synthase (nNOS) activity. Examples of indole- ketone include, but are not limited to, SU4312, SU5416, SU1 1248 (Sumtimb), and indirubm-3- oxime.
CN103720705A Cassava pharmacia haemostasis material and preparation method thereof The invention discloses a cassava pharmacia haemostasis material and preparation method thereof. The preparation method of cassava pharmacia provided by the invention comprises the following steps: mixing a cassava starch solution and a polyethylene glycol solution at 30 DEG C for 10 minutes for forming a water-in-water (W/W) emulsion, and controlling the stirring speed at 200-600 revolutions per minute; standing and incubating the W/W emulsion at 15-25 DEG C for 3-7 hours for centrifugation; cleaning, dehydrating and drying a lower layer gel solid for obtaining a white or light yellow cassava pharmacia. The raw material provided by the invention is a 'non-grain' biomass resource-cassava starch with wide source and low price, and the provided method has higher safety, and the prepared cassava pharmacia has better haemostasis effect.
WO2008091620A2 Combination therapy comprising romidepsin and i.a. bortezomib The invention provides a combination therapy for treating cancer and other neoplams including romidepsin and a proteasome inhibitor. When administered together, romidepsin and a proteasome inhibitor (e.g., bortezomib) interact synergistically to selectively kill malignant cells at low (nanomolar) concentrations. The effect is particularly pronounced in malignant hematological cells (e.g., leukemia, lymphoma, multiple myeloma). The combination has also been found useful in treating bortezomib-resistant cancers and steroid-resistant cancers. The invention provides methods of killing malignant cells in vitro and in vivo. Pharmaceutical compositions, preparations, and kits including romidepsin and a proteasome inhibitor are also provided.
CN101352419A Acebrophylline sugar-free type granular formulation and preparation method thereof The invention relates to an acebromine theophylline sugar-free granular agent and a preparation method thereof, in particular to a granular agent drug which takes the acebromine theophylline as active ingredients and a preparation method thereof, belonging to the western medicine formulation field; the acebromine theophylline sugar-free granular agent consists of the following ingredients by weight in every 1000 dose: 10 to 200g of acebromine theophylline materials, 400 to 4000g of diluents, 0 to 200g of disintegrating agents, 1 to 100g of adhesives, 5 to 300g of corrigents, 0 to 100g of solid fragrances and/or 0 to 200ml of liquid fragrances and 0 to 10g of colorants. The an acebromine theophylline sugar-free granular agent of the invention has the advantages of the use of the novel corrigent and the fragrance covers the self-bitter taste of the acebromine theophylline, avoids the use of sweeteners with a large quantity of sucrose, and the like, reduces the usage of excipients greatly, leads the packing quantity of single dosage of the preparation to be reduced obviously and leads the oral administration and taking of the medicine to be more convenient; simultaneously, the conversion problem of better dosage form of the acebromine theophylline materials is solved, especially the key problem of the stability of the granular agent; the production technique of the preparation of the invention is easy to realize production on scale extremely and is suitable to the national situation in China.
CN1660076A Preparation of slowly releasing silybum mariamum A slowlly-releasing silymarinum is prepared through preparing the dispersed solid silymarinum from PEG, PVP and Puliunike and preparing its inclusion compound by use of beta-CD or HB-beta-CD. Another process is also disclosed.
EP2271320A1 Raloxifene pharmaceutical formulations Pharmaceutical formulations comprising raloxifene or its salts, esters, polymorphs, isomers, hydrates, solvates, or derivatives thereof having defined particle sizes. Also described are processes for preparing formulations and methods of using such formulations.
CN101077418A Bacteria nano magnetosome loaded with primary amino medicine and preparation method thereof The present invention provides one kind of nanometer bacterial magnetic corpuscle carrying primary amino group medicine and its preparation process. The nanometer bacterial magnetic corpuscle consists of three structural units, including homotype double-function reagent, primary amino group medicine and nanometer bacterial magnetic corpuscle. The nanometer bacterial magnetic corpuscle carrying primary amino group medicine has high medicine carrying capacity, less aggregation, easy separation and purification, anticancer and antitumor effect similar to that of pure primary amino group medicine, but much lower toxicity.
CN103120699A Application of iridoid in preparation of anti-SARS (severe acute respiratory syndromes) medicines The invention provides application of iridoid with a general formula (I) in preparation of medicines for treating or preventing SARS (severe acute respiratory syndromes). R1 is selected from H, CH3, COOH or COOCH3; R2 is selected from H or OH; R3 is selected from H, OH, and OCOCH3; R4 is selected from H, OH or CH3; R5 is selected from H, CH3, OCOCH3, OH or CH2OH; R6 is selected from H, OH or CH3; and R7 is selected from H or OH. The IC50 (half maximal inhibitory concentration) value of compound 6 beta-hydroxyipolamiide is 138.8 muM, the IC50 value of compound shanzhiside methyl ester is 104.1 muM, and the IC50 value of compound 8-o-acetyl shanzhiside methyl ester is 125 muM.
CN102319259B 5% glucose adult nutrient solution and preparation method thereof The invention belongs to the technical field of medical drugs, and particularly relates to a 5% glucose adult nutrient solution and a preparation method thereof. The invention mainly solves the defects that some glucose injections cause great fluctuation of blood sugar and are easy to cause metabolic complications. The technical scheme of the invention is that the formula of the 5% glucose adult nutrient solution is that the following components are added into 100 mL of injection water: 5000 mg of glucose, 234 mg of sodium chloride, 128 mg of potassium acetate, 32.2 mg of magnesium acetate tetrahydrate, and 30 mg of sodium pyrosulfite; and the 5% glucose adult nutrient solution is prepared by concentrated preparation, diluted preparation, filling and sterilization. The 5% glucose adult nutrient solution of the invention has the advantages of complete metabolism, high energy supply, and less blood sugar fluctuation.
WO2007074707A1 THERAPEUTIC AGENT FOR NEUROBLASTOMA TARGETING ARID3b It is intended to provide a therapeutic agent for neuroblastoma. More particularly, it is intended to provide the therapeutic agent for neuroblastoma containing an ARID3b inhibitor.
CN102935086A Calcium tablet The invention discloses a calcium tablet. The calcium tablet contains 400-500mg of biological calcium carbonate, 120-140mg of xylitol, 100-120mg of glycine, 4-5mg of magnesium stearate, 4-5mg of non-dairy creamers, 4-5mg of citric acid, 0.1-1mg of natural pigment, 0.1-1mg of dextrin, 4-5mg of medical starches, 2-3mg of edible alcohol and 4-6mg of edible essence. According to the calcium tablet, the calcium content is high, bio-calcium which is commonly and easily available is adopted, the cost is low, and the great economical burden can not brought to a patient; the mouthfeel is good, and the mouthfeel of biological calcium carbonate is obviously superior to inorganic calcium carbonate; in addition, in the preparation process of the calcium tablet, the non-dairy creamers, the natural pigment, dextrin, citric acid and the like are added to adjust the taste, and different essences are added to prepare different flavors of calcium tablets; and the main points are as follows: the calcium tablet is quick in absorption and wide in applicable range.
WO2004062582A3 Combination therapy for anticoagulation A combination anticoagulation medicament including vitamin K with warfarin in an oral form is described. Between 50 and 5000 milligrams of vitamin K are combined in a single oral medication with 0.5 to 15 milligrams of warfarin for administration. The combination of vitamin K with warfarin in a single orally dosed form is a novel approach to improving the effectiveness of anticoagulation. The combination allows for broader application of warfarin in medical anticoagulation and reduces the variability of anticoagulation due to the influences of diet, additional medications, nutritional status, changes in physical condition, and potentially other factors. Use of the combination therapy improves the safety of warfarin as an appropriate anticoagulant for many medical conditions.
WO2008157393A1 Compositions comprising sulfide alone or in combination with nitric oxide and their use to The present invention provides methods of stimulating angiogenesis and the growth or migration of cells associated with angiogenesis, by contacting animals, tissues, or cells with sulfide, alone or in combination with nitric oxide. These methods may be used for a variety of purposes, including promoting wound healing, increasing blood flow, and for the treatment and prevention of diseases and disorders associated with decreased blood flow, including ischemic or hypoxic injury.
WO2008116107A3 Piperazine derivatives as glucokinase activators Compounds are provided for use with glucokinase that comprise the formula (I): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
EP2043663A1 Topical treatment of warts A method of treating common warts comprises topical administration of a pharmaceutical composition comprising dithionite in a pharmaceutically acceptable aqueous carrier to a wart, keeping the dithionite in the carrier in contact with the wart for a selected period of time so as substantially soften the wart, optionally repeating administration and contact, and mechanically removing the wart. Also disclosed is a medical patch comprising dithionite in a non-reducible matrix.
US20050080055 Method of treating breast cancer with androgen receptor antagonists This invention relates to the prevention and treatment of breast cancer in a subject, for example a female subject. Accordingly, this invention provides methods of a) treating a subject suffering from breast cancer; b) preventing, suppressing, inhibiting or reducing the incidence of breast cancer in a subject; c) delaying the progression of breast cancer in a subject suffering from breast cancer; d) preventing the recurrence of breast cancer in a subject; e) treating the recurrence of breast cancer in a subject suffering from breast cancer; and/or f) treating, preventing, suppressing or inhibiting metastasis in a subject suffering from breast cancer, by administering to the subject a therapeutically effective amount of an Androgen Receptor Antagonist and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, crystal, polymorph, prodrug or any combination thereof, as described herein.
US20110269756 Benzothiazolone derivatives Compounds of the formula I, in which R1, R2, R3, R3′, R4, R4′, E, E′, E″ and E′″ have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
CN102058633A External medicine for treating tinea unguium The invention discloses an external medicine for treating tinea unguium. The raw materials for preparing the external medicine for treating tinea unguium comprise acetic acid, impatiens balsamina, benzoate, sal-ammoniae, calomelas, sticky rice flour and salicylic acid. A preparation method of the external medicine comprises the following steps of: respectively grinding the impatiens balsamina, the benzoate, the sal-ammoniae, the calomelas, the sticky rice flour and the salicylic acid into fine powder which can pass a screen with 80-150 meshes, evenly mixing all the raw materials which are ground into the fine powder, adding 50% acetic acid to the evenly mixed raw materials and stirring evenly, and sealing up the evenly stirred mixture to obtain the external medicine for treating tinea unguium. The external medicine for treating tinea unguium has advantages of proportional and durable efficacy, good curative effects, low treatment cost and no toxic or side effects.
US20080275128 Contacting skin with X-ray contrast media such as iopamidol; sunscreen, cosmetics; colon disorders Embodiments of the invention relate to methods and compositions for treating symptoms related to inflammatory conditions and to methods and compositions for treating inflammatory components of common cold, utilizing various method of administration of X-ray contrast media (CM).
EP2203445A1 Azabicyclo ý3. 1. o¨hexyl derivatives as modulators of dopamine d3 receptors The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5, and n is 1 or 2; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
WO2014036429A1 Mirna modulators of chronic visceral inflammation Provided are methods for the modulation of chronic visceral inflammation in a cell, tissue, organ and/or subject using miRNA agents. Also provided are miRNA agents (e.g., miRNA, agomirs, and antagomirs) that can modulate the level of chronic inflammation and methods of screening for such agents. Also provided are compositions (e.g., aptamirs or exomirs) that facilitate cell/tissue-specific delivery of the miRNA agents.
CA2153570C Pharmaceutical composition for treating nicotine dependence Galanthamine, as well as its pharmaceutically acceptable acid addition salts, is used to treat nicotine dependence. The active substances are released orally, transdermally or in any other parenteral manner from pharmaceutical compositions in a continuous and controlled way.
CN102379919A Epidemic prevention pellet The invention relates to an epidemic prevention pellet. A preparation method of the epidemic prevention pellet comprises the following steps of: grinding liquoric root, wild ginger, dahurian angelica root, menthol crystal and borneol into fine powder; uniformly mixing with added cool boiled water; twisting into pills; grinding cinnabar into fine powder; and uniformly coating on the outer layer of the pills. The epidemic prevention pellet is easy to prepare, is economic and practical, has a remarkable effect, and can be used for improving the human body immunity, effectively preventing the overflow of an epidemic situation, and treating headache, toothache and whole body arthralgia.
US20120082621 Swallowtail motifs for imparting water solubility to porphyrinic compounds Porphyrinic compounds that contain solubilizing groups are described, along with methods of making and using the same and compositions comprising such compounds. Examples of such compounds include compounds compounds of Formula I: wherein: Z is a porphyrinic macrocycle, Alk1 and Alk2 are each independently an alkylidene chain; L is a linking group or is absent; R1 is preferably an ionic group or polar group; R2 is an ionic group, polar group, bioconjugatable group, or targeting group; R3 is present or absent and when present is a halo group, bioconjugatable group, or targeting group, n is O or 1 (that is, the CH group is present, or Alk1 and Alk2 are bonded directly to a carbon of the porphyrinic macrocycle Z); or a salt thereof.
WO2009083940A3 Processes for the preparation of 2,5-dihydroxybenzenesulfonic acid salts Processes for the preparation of 2,5-dihydroxybenzenesulfonic acid salts of formula (I) and a crystalline form of potassium 2,5 2,5-dihydroxybenzenesulfonic acid are provided.
US20100260823 Preparation with marine collagen for protease inhibition The invention relates to pharmaceutical preparations made from marine collagens for inhibiting matrix metalloproteases and the use of a marine collagen for production of a pharmaceutical preparation for inhibiting matrix metalloproteases.
WO2008071010A1 Combination treatments with selected growth/hormone regulatory factors for diabetes and related diseases The invention relates to compositions, conjugates, and methods for the prevention and/or treatment of a condition and/or disease comprising a therapeutically effective amount of at least one EGF receptor ligand, at least one GLP-1 agonist, and preferably one or more of at least one gastrin compound and at least one gastrin agonist. The combination of at least one EGF receptor ligand, at least one GLP-1 agonist, and one or more of at least one gastrin compound and at least one gastrin agonist provides beneficial effects, in particular sustained beneficial effects, in the prevention and/or treatment of conditions and/or diseases including but not limited to diabetes, hypertension, chronic heart failure, fluid retentive states, obesity, metabolic syndrome and related diseases and disorders. Combinations of at least one EGF receptor ligand, at least one GLP-1 agonist, and preferably one or more of at least one gastrin compound and at least one gastrin agonist can be selected to provide unexpectedly additive, complementary or synergistic effects.
US20100291151 1-methylpyrazole modulators of substance p, calcitonin gene-related peptide, adrenergic receptor, and/or 5-ht receptor The present invention relates to new 1-methylpyrazole modulators of substance P release, calcitonin gene-related peptide activity, adrenergic receptor activity, and/or 5-HT receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
CN101822690A Composition of dextran 40 and sodium lactate Ringer' solution and preparation method The invention relates to a composition of dextran 40 and sodium lactate Ringer' solution, which contains the following components by weight ratio: 25kg of dextran 40, 1500g of sodium chloride, 50g of calcium chloride, 75g of potassium chloride, proper amount of sodium lactate, proper amount of hydrochloric acid or sodium hydroxide, and 250L of water for injection. And a preparation method of composition of the dextran 40 and sodium lactate Ringer' solution comprises the following steps: (1) dissolving prescribed amount of dextran 40, sodium chloride, calcium chloride, potassium chloride and sodium lactate in the water for injection; (2) adding 0.04% (g/ml) active carbon for needle according to the liquid preparation quantity, lowering the temperature, filtering the active carbon, regulating the pH value to be 5.0-7.5, filtering through a 0.45mu m filter membrane, and cycling for 15min; and (3) sampling and measuring the pH value and the content, encapsulating after being qualified, and hot-pressing and sterilizing at 115 DEG C for 30min.
CN103044254A 2,4-dyhydroxy-6-substituted-phenyl aliphatic ketone derivatives and application thereof The invention discloses 2,4-dyhydroxy-6-substituted-phenyl aliphatic ketone derivatives and application thereof in preparation of gram negative pathogen resistant inhibitor. Tests confirm that the 2,4-dyhydroxy-6-substituted-phenyl aliphatic ketone derivatives have the effect of obviously inhibiting the type III secretion system of gram negative bacteria; the inhibitors do not inhibit growth of salmonella typhimurium, but is capable of inhibiting invasion of salmonella typhimurium to the host cell, and therefore, the inhibitors can be applied as the type III secretion system inhibitors for gram negative bacteria; and furthermore, the inhibitors can be used as anti-bacterial virulence factor preparations for preparing gram negative pathogen resistant medicines.
CN101084880B Biological solid dispersion of vitamin E esters derivatives and preparation method thereof The invention relates to a solid dispersion of insoluble medicinal vitamin E esters derivant such as vitamine E nicotinate, acetic ester and succinic ester and its preparation method. The dissolving velocity in vitro and absorption eegree in vivo of the vitamin E esters derivant is remarkably improved after being treated by solid dispersion.
CN101675995A 10-hydroxycamptothecinreagent-delivery lipid ultrasound microbubble agent and its preparation method The invention provides a 10-hydroxycamptothecinreagent-delivery lipid ultrasound microbubble agent, characterized in that the lipid ultrasound microbubble agent is prepared by encapsulating biologicalinert gas with a bilayer lipid membrane, 10-hydroxycamptothecin is encapsulated in a bilayer, the bilayer lipid membrane is prepared from the following raw materials based on the part by weight: 2 to3 parts of 10-hydroxycamptothecin, 7 to 9 parts of phosphatide mixture and 0.1 to 0.5 part of nonionic surfactant. The ultrasound microbubble can enhance the ultrasonic development, is mainly used for supporting a drug carrier of 10-hydroxycamptothecin, can protect a-hydroxyl lactone ring structure with the antitumor activity, and can be destroyed by the treating ultrasound at the specific position under the monitoring condition with the ultrasound in the targeting way to release 10-hydroxycamptothecin, thereby reaching the purpose of improving the curative effect and reducing the toxic and side effect. The invention also relates to a method for preparing the drug-delivery ultrasound microbubble, characterized in that a mechanical oscillation method is adopted, the microbubble prepared bythe method has high yield, stable performance and good development effect, a small amount of phosphatides are used, and the drug entrapment rate and the drug-delivery amount are high.
CN1903180A Freeze-dried powder injection of frusemide and its prepn. method A powder injection of frusemide is prepared from frusemide, mannitol or saccharide, NaOH (or meglumine) solution and hydrochloric acid through freeze drying. Its preparing process is also disclosed.
CN102335175A Medicament for removing onychomycosis The invention relates to a medicament for removing onychomycosis. The invention provides a medicament for removing onychomycosis, and the medicament is prepared by uniformly mixing itraconazole and vaseline based on a proportion that every 10 to 20mg of itraconazole raw material is mixed with 10g of vaseline. According to the medicament for removing onychomycosis, the unique efficacy of sporanox in treating onychomycosis is sufficiently utilized, the medicament is prepared into an external preparation, and the complicated side effect of the medicament serving as an oral medicament can be avoided. The medicament has the advantages of good treatment effect, short course of treatment, less side effect and convenience in use.
CN102166189A Target and fluorescence dual-functional slightly-soluble antitumor medicament nano structural lipid carrier The invention relates to the field of medicinal preparations, in particular to a target and fluorescence dual-functional slightly-soluble antitumor medicament nano structural lipid carrier. In the slightly-soluble antitumor medicament nano structural lipid carrier, a lipid carrier of which the inside carries medicaments is formed by solid lipid, liquid lipid, surfactants and slightly-soluble antitumor medicaments; and the surface of the lipid carrier is chemically modified and is in covalent connection with a ligand with a tumor target. The slightly-soluble antitumor medicament nano structural lipid carrier can prolong the in-vivo circulation time of the slightly-soluble antitumor medicaments and improve the bioavailability of the slightly-soluble antitumor medicaments and can be used fortopical diagnosis of tumors by fluorescence imaging.
WO2014128209A1 Pharmaceutical formulation comprising dpp-iv inhibitor agglomerates The invention relates to a pharmaceutical formulation comprising DPP-IV inhibitor agglomerates and/or DPP-IV inhibitor particles, wherein the DPP-IV inhibitor is in free form or in form of a salt thereof, wherein at least 45 wt.% of the DPP-IV inhibitor particles and/or DPP-IV inhibitor agglomerates have a size when measured using sieve analysis of more than 250 μm. The pharmaceutical formulation shows improved process stability and allows easy production of solid oral dosage forms due to the good flow properties of the particles and/or agglomerates.
CN103623003A Pearl eye drops for improving eyesight and preparation method thereof The invention discloses pearl eye drops for improving eyesight and a preparation method thereof. Particularly, butanediol is added to the prescription of the preparation, so that dry eyes are effectively relieved, and stimulus response caused by ethanol in the traditional formula can be reduced. Thus, the side effect of the medicine is reduced.
WO2013041407A1 Hydroxamic acids as hdac6 inhibitors A hydroxamic acid of formula (I) or a pharmaceutically acceptable salt thereof for use in a method for treating or preventing an immunological, inflammatory, autoimmune or allergic disorder or disease, or a transplant rejection, or a graft-versus host disease, or a neurogenerative disease, or neuron injury, where the symbols in formula (I) have the following meanings: X is aryl, heteroaryl, cycloalkyl or heterocyclyl, any of which is unsubstituted or substituted, or H; L is C1-C14 saturated alkylene or C2-C8-alkenylene, wherein the alkylene or alkenylene is unsubstituted or substituted, wherein one or two of the carbon atoms of the alkylene or alkenylene is replaced by NR', R' being hydrogen, alkyl, acyl, hydrogen, arylalkyl or, together with R, is (C1-C3)-alkylene, and wherein one or two of the carbon atoms of the alkylene or alkenylene is optionally replaced with O, S, S(O), S(O)2 or C(O); and R is H or, together with R', (C1-C3)-alkylene.
EP2567959A1 6-(4-Hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula, in which R1, R2, R3, R4 and R5 are defined as indicated below. The compounds of the formula are kinase C (PKC) inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
US20060160810 2-Alkoxyphenyl substituted imidazotriazinones The 2-phenyl-substituted imidazotriazinones having short unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolising phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for treating cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for treating erectile dysfunction.
US20120095083 Use of triplex structure dna in transferring nucleotide sequences A method to induce an immune response in a host in need thereof, comprises administering to the host, recombinant lentiviral vector particles comprising: a) a GAG polypeptide or a functional GAG-polypeptide derivative; b) a POL polypeptide or a functional POL-polypeptide derivative ; c) an ENV polypeptide or a functional ENV-polypeptide derivative; and d) a recombinant polynucleotide. The recombinant polynucleotide comprises a transgene placed under the control of regulatory signals for transcription and expression, regulatory signals, of lentiviral origin, for reverse transcription, expression and packaging, and a polynucleotide comprising a cis-acting central initiation region (cPPT) and a cis-acting termination region (CTS). The regions are of lentiviral origin and are inserted in a functional orientation with the regulatory signals of lentiviral origin. The polynucleotide forms a DNA triplex during reverse transcription.
CA2656807A1 Early detection and prognosis of colon cancers A genome wide microarray gene expression approach for human colorectal cancer cells was used to identify hundreds of hypermethylated genes for colon cancer. We compared isogenic cells altered pharmacologically versus genetically to induce genomic demethylation, to pinpoint genes activated by DNA demethylation, but not by inhibition of class I and II histone deacetylases (HDACs). We achieve an 82% success rate in predicting genes with densely hypermethylated CpG islands and complete gene silencing. The genes are similarly hypermethylated in primary tumors and have previously undetected tumor suppressor functions. The genes can be used diagnostically to detect cancer, pre-cancer, and likelihood of developing cancer.
CA2557307A1 3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis c virus ns3 serine protease The present invention discloses novel compounds according to formula (I) which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease. Wherein: R1 is H, OR8, NR9R10, wherein R8, R9 and R10 can be the same or different, each being independently selected from the group consisting of H, alkyl-, alkenyl-, alkynyl-, aryl-, heteroalkyl-, heteroaryl-, cycloalkyl-, heterocyclyl-, arylalkyl-, and heteroarylalkyl, or alternately R9 and R10 in NR9R10 are connected to each other such that NR9R10 forms a four to eight-membered heterocyclyl, and likewise independently alternately R9 and R10 in CHR9R10 are connected to each other such that CHR9R10 forms a four to eight-membered cycloalkyl; Y represents a group G-R wherein G is NH or O.
EP1251850B1 Use of a combination preparation in cancer therapy A method for treating a human patient afflicted with cancer, is provided in which therapeutically effective amounts of temozolomide and irinotecan are administered to such a patient. Also provided is a medical kit comprising: (a) a supply of temozolomide; (b) a supply of irinotecan; and (c) printed instructions for administering temozolomide and irinotecan to a cancer patient.
EP1867335A2 Formulations with angiogenesis-dependent tumour action The use of defibrotide and/or oligodeoxyribonucleotides having a molecular weight of 4000-10000 Dalton as an anti-tumour agent in combination with rapamycin, is described. The oligotide may be produced by extraction from animal and/or vegetable tissues, in particular, from mammalian organs, or may be produced synthetically. The tumors which can be treated are preferably angiogenesis-dependent tumors, such as multiple myeloma or breast carcinoma.
WO2012170664A3 Methods of cancer treatment and prevention through the modulation of sirt4 activity The present invention relates to methods of preventing or treating cancer through the use of agents that enhance the activity or expression of SIRT4.
US7399772 Substituted benzimidazole dosage forms and method of using same The present invention relates to pharmaceutical preparations comprising substituted benzimidazole proton pump inhibitors. There is provided a liquid or solid pharmaceutical composition consisting of a proton pump inhibitor and at least one buffering agent. Also provided is a pharmaceutical composition further comprising a parietal cell activator, an anti-foaming agent, a flavoring agent and combinations thereof; a method for treating acid-related gastrointestinal disorders by administering a solid pharmaceutical composition; and, a kit for the preparation of a liquid oral pharmaceutical composition. Dosage forms include: liquid, powder, tablet, capsule, effervescent powder, effervescent tablet, pellets, and granules.
EP2065047A1 Methods of enhancing the therapeutic activity of NSAIDS and compositions of zwitterionic phospholipids useful therein Disclosed are compositions comprising non-steroid anti-inflammatory drugs (NSAID's) complexed with zwitterionic, neutral phospholipids, or both, having reduced gastrointestinal irritating effects and enhanced anti-pyretic, analgesic, and anti-inflammatory activity. Also disclosed are improved methods of using the complexes for treating fever, inflammation, and preventing platelet aggregation. In some embodiments, the anti-pyretic activity of sub-therapeutically used amounts of NSAID's are enhanced to elicit anti-pyretic activity in vivo when associated (noncovalently) with zwitterionic phospholipids, such as dipalmitoyl phosphatidyl choline.
WO2013189219A1 Xanthine derivative Disclosed are a xanthine derivative having the structure of the following general formula (I) or pharmaceutically acceptable salts thereof; further disclosed is a preparation method for the xanthine derivative or pharmaceutically acceptable salts thereof; and further disclosed is the use of the xanthine derivative or pharmaceutically acceptable salts thereof. Through experiments of influence of in-vitro DPP-IV activity inhibition experiments on glucose tolerance of normal mice and on blood glucose of mice with spontaneous diabetes, it proves that the compounds and pharmaceutically acceptable salts thereof show good DPP-IV inhibition activity, can be applied to prepare medicines in the medicines for treating dipeptidyl peptidase IV-related diseases, and more particularly, can be applied to the use of medicines for treating type II diabetes or diseases of abnormal glucose tolerance.
EP1883412A1 Combination therapy with sulodexide and a blood pressure reducing agent in the treatment of diabetic nephropathy The present invention is directed to a method of treating patients suffering from nephropathy of diabetic origin by administration of sulodexide in combination with a blood pressure reducing agent, such as an inhibitor of an angiotensin converting enzyme (ACE inhibitor) and/or with an angiotensin II receptor blocker (ARB). The effectiveness of sulodexide with an ACE inhibitor or an ARB has been shown by the significant decrease of the albuminuria in microalbuminuric diabetic patients.
CN1807435A Water soluble phosphate ester salt ofú¿Zú®-3'-hydroxy-3,4',5-trimethoxydiphenyl ethylene, and its preparation method ,pharmaceutical composition and uses The invention relates to the compound of formula (1), among it, M denotes K+, Na+ or NH4+; it also relates to Process for preparing, medicinal composition and application in the treatment of antineoplastic endothelial cell and resistant blood vessel proliferation. The Process for preparing is (Z)-3'-hydroxyl-3, 4', 5- trimethyl diphenyl ethylene and phosphorylating agent react in the existence of acid- attach agent to generate phosphorylating intermediate, then getting the product afer the reflux in queous alkali. The compound of formula (1) not only hasing good inhibited activity to multiple tumour cell strain's growth, but also combining with microtubulin in tumour endothelial cell, restraining polymerization, stopping karyokinesis, leading to the clogging of blood vessel which providing oxygen and nutrient for tumour, exerting target antivasal action amd making tumour cell die because of lack of blood. In addition, the endothelial cell of abnormal propagation can be peeled because of the change of morphology in low concentration. Hence, the compound of formular (1) can be used to prevention and cure of tumour and antivasal hyperplasia.
WO2008146063A1 New benzofuran derivatives as selective 5ht6 receptor inhibitors and process for their preparation The present invention relates to new selective 5HT6 receptor binding benzofuran derivatives of general formula (I) wherein, Z represents a hydrogen atom, C1-4 acyl group, C1-6 alkyl sulfonyl group, phenyl sulfonyl group substituted with one or more halogen atom; or naphthyl sulfonyl group optionally substituted with a halogen atom, tetrahydro naphthyl sulfonyl group, (lS)(+)-10-camphor-sulfonyl group, (lR)(-)-10-camphor-sulfonyl group or benzofuranyl sulfonyl group, substituted with a halogen atom and C1 -4 alkyl group, Y represents C2-6 alkylene group, R1 and R2 represent, independently, a hydrogen atom, C1-4 alkyl group, benzyl group, or together with one or more halogen atoms, trifluoromethyl group, or C1-4 alkoxy group substituted 4-phenyl-piperazine-l-yl group; and/or their pharmaceutically suitable acid addition salts, to the process for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in treatment and/or prevention of disorders of the central nervous system and cardiovascular system.
US20120015983 Synthesis and Novel Salt Forms of (R)-3-((E)-pyrrolidin-3-yl)vinyl)-5-tetrahydropyran-4-yloxy)pyridine The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions.
US8623922 Bronchodilating Beta-agonist compositions and methods Bronchodilating compositions and methods are provided. The compositions are intended for administration as a nebulized aerosol. In certain embodiments, the compositions contain formoterol, or a derivative thereof. Methods for treatment, prevention, or amelioration of one or more symptoms of bronchoconstrictive disorders using the compositions provided herein are also provided.
US20120100184 Synthesis of 1-amino-1,3,3,5,5,-cyclohexane mesylate Process for manufacturing 1-amino-1,3,3,5,5-pentamethylcyclohexane mesylate comprising step (i): (i) reacting 1-amino-1,3,3,5,5-pentamethylcyclohexane with methane sulfonic acid in a solvent or a mixture of two or more solvents selected from anisole, cumene, pentane, hexane, heptane, isooctane, methyl acetate, propyl acetate, isopropyl acetate, n-butyl acetate, isobutyl acetate, methyl ethyl ketone, methyl isopropylketone, methyl isobutyl ketone, dimethyl sulphoxide, tetrahydrofuran, methyltetrahydrofuran, 1,1-diethoxypropane, 1,1-dimethoxymethane, and 2,2-dimethoxypropane.
WO2012003704A1 Sodium alginate crosslinked slow-released moxiflorxacin microsphere, the preparation method and the use thereof, and target vascular occlusive agent of the microsphere A sodium alginate crosslinked slow-released moxifloxacin microsphere, the preparation method of the microsphere, a vascular target embolus containing the microsphere and the use of the microsphere in preparing the vascular target embolus. The microsphere contains moxifloxacin, a drug carrier, a adsorbent, a reinforcing agent and a solidifying agent, wherein the drug carrier is sodium alginate, the adsorbent is albumin prepared from human plasma or bovine serum albumin, the reinforcing agent is gelatin or hyaluronic acid, and the solidifying agent is a divalent metal cation chosen from calcium salt or barium salt.
WO2008086739A1 Use of ursolic acid saponin, oleanolic acid saponin in preparation of increasing leucocyte and/or platelet medicine The invention provides use of ursolic acid saponin, oleanolic acid saponin of formula (I) in preparing medicine for increasing leucocyte and/or platelet. The invention also provides a composition containing compound of formula (I). The invention utilizes ursolic acid and oleanolic acid as raw material which are widely presented in natural products and cheap and easy to get, introduces glycosyls or oligosaccharyls by structural modification. It is proved that the compounds of formula (I) have the action of obviously increasing leucocyte and/or platelet by pharmacological tests.
DE102006060953A1 Synergistic preparation for treating urinary tract inflammation, e.g. cystitis, contains low molecular hyaluronic acid and another glycosaminoglycan, preferably chondroitin sulfate A pharmaceutical preparation (I) contains effective amounts of (a) hyaluronic acid and/or its salts (preferably of average molecular weight less than 200 kDa) and (b) other glycosaminoglycan(s) (preferably chondroitin sulfate(s)). - ACTIVITY : Antiinflammatory; Uropathic. A composition containing sodium hyaluronate (a') of non-animal origin (average molecular weight 180 kDa) and chondroitin sulfate (b') of marine origin (each at 40 mg per 50 ml) was instilled into the bladder of interstitial cystitis patients once per week for 2 months. The average subjective effectiveness at the end of the therapy (on a scale of 1 = very good to 6 = inadequate) was 2.0, compared with 3.1 after treatment with (a') only, 3.3 after treatment with (b') only and 4.8 after placebo treatment. Cytoscopic studies showed that in the group treated with both (a') and (b') the bladder mucosa was almost completely intact, with no lesions or bleeding. - MECHANISM OF ACTION : Protection, reduction of permeability and regeneration of urinary tract mucosa.
CN102961413A Compound Yunnan Baiyao enema and preparation method thereof The invention discloses compound Yunnan Baiyao enema. The compound Yunnan Baiyao enema comprises Yunnan Baiyao, furazolidone, dexamethasone acetate, epinephrine hydrochloride, procaine hydrochloride, carboxymethyl cellulose sodium and distilled water. The compound Yunnan Baiyao enema is reasonable in prescription, and has a remarkable effect on treating factitial proctitis.
US20120027819 Medical Devices Incorporating a Bioactive and Methods of Preparing Such Devices One embodiment provides a medical device comprising a base material and a bioactive in contact with the base material, the bioactive having a proton binding site with a non-ionic form and an ionic form, the bioactive being less soluble in water when the proton binding site is in the non-ionic form than when the proton binding site is in the ionic form, wherein at least 5% w/w of the bioactive is present with the proton binding site in the non-ionic form and wherein the bioactive is not an anesthetic. Another embodiment provides such a medical device where the bioactive is an anesthetic and where the device is not a ureteral stent. Another aspect provides method of manufacturing such devices.
CN101161688A Novel process for synthesizing povidone iodine by gas phase/ solid phase reaction The present invention discloses a novel process for synthesizing povidone iodine by gas phase and solid phase reaction. The process combines the iodine-subliming purification process and the synthesization process of povidone iodine by using periston and coarse iodine as raw materials, using a gas phase-solid phase reactor for synthesizing povidone iodine, heating the coarse iodine in the iodine sublimation kettle to make it to sublime to be purified, leading the iodine steam through the heat-preserving conduit into the gas phase-solid phase reactor containing the solid periston to perform gas phase and solid phase reaction directly; adding inert gases with a certain velocity of flow and volume of flow in iodine sublimation kettle to take and raise the flow of the iodine steam in to the gas phase-solid phase reactor; controlling gas phase-solid phase reactor to rotate clockwise and counter-clockwise in a predetermined cycle, and keeping a certain reaction temperature to make periston and iodine stream to be contacted, adsorbed and reacted adequately; exhausting after treatment of the exhaust gas which is connected to the collecting pot of the exhaust gas by the exhaust pipe; batching off when reacting the schedule time to obtain the povidone iodine meeting the pharmacopoeia standard.
WO2014090715A1 Thiazole derivatives as inhibitors of bruton's tyrosine kinase This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
WO2014096464A1 Pharmaceutical composition comprising leflunomide The present invention relates to a pharmaceutical composition according to the invention containing 14 to 17.5 mg leflunomide prepared as a single dose and uses thereof.
US20080090878 Pharmaceutical combinations and their use in treating gastrointestinal and abdominal viscera disorders The present invention relates to a combination of a first agent including either a 5-HT4 receptor agonist or antagonist or a 5-HT3 receptor antagonist and a co-agent and pharmaceutical compositions and formulations containing the combination. The present invention also relates to a method of treating a gastrointestinal and abdominal viscera disorder by administering the pharmaceutical compositions to a patient. The pharmaceutical compositions may also be employed as laxatives, to prepare a patient for colonoscopy and to regulate and stabilize enterochromaffin cell secretory, pain and motility mechanisms, afferent fiber activity and GI and lower abdominal smooth muscle cells. The dosage is preferably oral and administration is preferably once or twice a day. The preferred first agent is tegaserod.
CN103408501A Benzyl pyrimidine derivatives, and preparation method and medical application thereof The invention relates to the field of pharmaceutical chemistry, specifically to benzyl pyrimidine derivatives (I), preparation methods thereof, medicinal compositions containing the derivatives and medical application of the derivatives, in particular, application of the derivatives as an immunosuppressant in autoimmune diseases and organ transplantation.
WO2012142372A2 Compositions and methods for the treatment of nasal conditions The invention provides compositions and methods for treating nasal congestion. The provided compositions and methods utilize iow concentrations of selective a-2 adrenergic receptor agonists. The compositions preferably include brimonidine.
CN1857237A New use of falcarindiol The present invention discloses the application of falcarindiol in preparing antiphlogistic and analgetic medicine.
CN101284125A Attapulgite water-based kibe formulations The invention discloses an attapulgite water-based chilblain preparation, which is prepared from purified attapulgite clay, extractive solution of red pepper, extractive solution of safflower, extractive solution of purple garlic, extractive solution of ginger, extractive solution of pricklyash peel, extractive solution of notoginseng, borneol, potassium sorbate, and honey by mixing, stirring at high speed to obtain suspension, and canning. The chilblain preparation employs purified attapulgite clay as suspending agent to increase chilblain preparation adhesion, and improve pharmaceutical usage effect; and has the effects of promoting the flow of qi by warming the channel, promoting blood circulation, decreasing swelling, inhibiting inflammation, relieving pain, and abating skin pruritus. The chilblain preparation has small irritation to skin and can be used for preventing and treating slight chilblain.
CN103462942A Suction-type ambroxol hydrochloride solution The invention discloses a suction-type ambroxol hydrochloride solution. The suction-type ambroxol hydrochloride solution is characterized in that per 100 mL of menstruum contains 0.15-0.3 g of ambroxol hydrochloride, a surface active agent accounting for 4-6 percent of the ambroxol hydrochloride in mass and a right amount of antioxidant and antiseptic; the pH value of the solution is 4.6-5.8; the menstruum is selected from water for injection, physiological saline and isotonic glucose solution. The suction-type ambroxol hydrochloride solution is sprayed into a patient's mouth, forms mist, directly enters a respiratory tract, is high in suction rate and local condition, realizes the safe and target treatment purpose, and effectively prompts the patient's phlegm to be discharged. Moreover, the suction-type ambroxol hydrochloride solution is low in use amount, high in medical effect, safe, good in stability, low in probability of pollution or oxidative deterioration and long in shelf life.
US20110009463 Geranylgeranyl transferase inhibitors and methods of making and using the same The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.
WO2012138669A1 Solid state forms of hiv inhibitor The invention relates to novel crystalline forms of (2S)-2-tert-butoxy-2-(4-(2,3- dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid, the hydrochloride salt thereof, novel crystalline forms of the hydrochloride salt, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection.
CN101385736A Use of penoniflorin in preparing medicine for preventing and treating depression and medicine composition thereof The invention relates to an application of paeoniflorin in drugs for preventing and treating depression and a pharmaceutical composition thereof, and the pharmaceutical composition contains effective dose of the paeoniflorin and a pharmaceutical acceptable carrier. The pharmaceutical composition can be prepared into various conventional liquid formulations or solid formulations. The paeoniflorin is proved to have better efficacy for the depression and long duration of the efficacy through a rat forced swimming test, a open field test and a new environment feeding inhibition test. The drugs which take the paeoniflorin as an active ingredient and are used for treating and preventing the depression have good effects, long duration, insignificant toxicity and side effect and low price.
US20100331409 Use of Methyl Cinnamate in the Inhibition of Candida Albicans Biofilms The invention provides a method of inhibiting biofilm formation or development of Candida albicans, comprising applying to an object in need thereof an effective amount of methyl cinnamate whereby formation or development of Candida albicans biofilm can be inhibited or prevented. Also provided is a method of treating Candida albicans biofilm-associated infections, comprising administrating to a subject in need thereof a therapeutically effective amount of methyl cinnamate.
WO2007084162A3 Sirtuin inhibiting compounds Provided herein are compositions and methods for treating or preventing cancer and autoimmune diseases. Compositions comprise a sirtuin inhibitory compound that decreases the activity of a sirtuin, such as SIRTl or Sir2. Exemplary methods comprise contacting a cell or a molecule with a sirtuin inhibitory compound that decreases the activity of a sirtuin and thereby reduces the life span of a cell, kills the cell or renders it suspectible to certain cell stresses including radiation and chemotherapy. Other methods include treating pathogens expressing a sirtuin.
US8247402 Crystal form of pyrrolidylthiocarbapenem derivative Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)p yrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2θ) of about 13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees) and a crystal of said compound having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2θ) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.
CN103484345A Formula and production method of lucid ganoderma wine for clearing heat and improving hearing A formula and a production method of a lucid ganoderma wine for clearing heat and improving hearing. Raw materials comprise lucid ganoderma, coptis, evodia, root of large-flowered skullcap, balloonflower root, fructus forsythia, isatis root, Lasiosphaera seu Calvatia, burdock, mint, Mirabilitum, licorice, kernel of Gardenia jasminoides, mint leaf and fructus forsythia. The production method comprises a main process flow containing material selection, drying, material blending, immersion, packaging and finished product acquisition. The wine combines efficacies of soothing the nerves, tranquillizing, clearing heat, detoxifying, nourishing liver, tonifying kidney, dispelling wind and radiating heat, has the advantages of delicious taste, convenience for usage, pure natural materials, no toxic or side effect, and is suitable for drinking in hotels and households.
US20100255061 Posterior Segment Drug Delivery A therapeutic device to release a therapeutic agent comprises a porous structure coupled to a container comprising a reservoir. The reservoir comprises a volume sized to release therapeutic amounts of the therapeutic agent for an extended time when coupled to the porous structure and implanted in the patient. The porous structure may comprise a first side coupled to the reservoir and a second side to couple to the patient to release the therapeutic agent. A plurality of interconnecting channels can extend from the first side to the second side so as to connect a first a plurality of openings on the first side with a second plurality of openings on the second side. Each of the openings on the first side can be connected to each of the openings on the second side with the plurality of interconnecting channels, such that the rate of release of the therapeutic agent can be substantially maintained when one or more of the openings is blocked, for example with particles, cells, bacteria or tissue when the device is implanted for an extended time. The length of the channels extending from the first side to the second side may comprise an effective length greater than a distance across the porous structure from the first side to the second side. The therapeutic device many comprise an expandable retention structure and an expandable reservoir, such that the device can be delivered from a lumen of a delivery device and expand when positioned in the patient. The therapeutic device may comprises a penetrable barrier to inject therapeutic agent into the device when implanted in the patient.
CN101190195A N-acethy aminophenol chewable tablets for dog or cat The invention discloses an acetaminophen chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the existing tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 30 to 50 percent of acetaminophen.
EP2085082A1 Treatment of cognitive decline The present invention relates to the treatment of decline of cognitive functions, and particularly it relates to the use of medium chain dicarboxylic acids as medicament or a dietary integrator for the treatment of decline of cognitive functions. The dicarboxylic acids according to the present invention have the following formula: HOOC-(CH2)n-COOH, wherein n is an integer ranging from 6 to 16 or pharmaceutically acceptable salts, derivatives or mixture thereof.
CN1562078A Medicine for treating beri-beri A medicine for treating beriberi is prepared from 10 raw materials including borneol, realgar, sulfur, chlorpheniramine, benadryl, griseofulvin, VB1, etc.
CN101912384B Application of flavone lignan to preparing medicaments for treating virus B hepatitis The invention relates to application of flavone lignan to preparing medicaments for treating virus B hepatitis, in particular to (+/-)-2-[2,3-dihydro-3-(3,5-dimethoxy-4-hydroxyphenyl)-2-methylol-1,4-benzodioxane-6]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-ketone or application of medicinal salts thereof to preparing medicaments for treating the virus B hepatitis or preparing medicaments forreducing virus B hepatitis surface antigens (HBsAg). Because the flavone lignan has high-efficiency activity for suppressing the HBsAg, the flavone lignan can be expected to be applied to preparing medicaments for treating the virus B hepatitis.
CN101993439A Lamivudine crystal form and preparation method thereof The invention relates to lamivudine crystal form and a preparation method thereof. Under the Cu-Ka radiation, the characteristic peaks of the lamivudine crystal form IV of the invention appear on the crystal X-ray powder diffraction pattern at the following reflection angle 2 theta: 9.7+/-0.2, 10.02+/-0.2, 11.24+/-0.2, 11.52+/-0.2, 12.80+/-0.2 and 13.10+/-0.2.
US20110123625 Compositions of Less Immunogenic and Long-Circulating Protein-Lipid Complexes Provided are lipidic particles comprising phosphatidylcholine, phosphatidylinositol and cholesterol. Also provided are compositions comprising the lipidic particles and having associated therewith therapeutic agents such as peptides, polypeptides or proteins. In these compositions, the therapeutic agents have reduced immunogenicity and/or longer circulating time. These compositions can be used for therapeutic administration of the peptides, polypeptides and/or proteins.
CN101219142A Method for preparing small-molecule antineoplastic medicament with specificity for CYP2J2 and medical use thereof The invention relates to a preparation method and pharmacy applications of small molecular antitumor drug with specificity aiming at CYP2J2, which belongs to antitumor drugs and biochemical reagents. The general formula of the structure of the invention is 1-[4-phenyl]-4-[4-(diphenyl hydroxymethyl)-piperidyl]-butanone hydrochloride. The product of the invention is white or grey white powder, which can be dissolved in water or ethanol but hardly dissolved in aether; the melting point thereof is 208 to 210 DEG C. The invention also can be used as an inhibitor to inhibit the activity of CYP2J2 enzyme in pharmaceutical applications.
US20100150839 Compositions and Methods for Modulating Cognitive Function The present invention provides compositions and methods for modulating, e.g., enhancing, cognitive function. The methods involve modulation of translation, modulation of a MAPK signaling pathway, or both. The invention further provides screening methods useful in identifying compounds that modulate, e.g, enhance, cognitive function. The invention further provides method of treating a subject to modulate cognitive function.
US7195870 Diagnosis of diseases associated with gene regulation Chemically modified genomic sequences of genes associated with gene regulation, to oligonucleotides and/or PNA-oligomers for detecting the cytosine methylation state of genes associated with gene regulation which are directed against the sequence are disclosed. In addition, a method for ascertaining genetic and/or epigenetic parameters of genes associated with gene regulation is disclosed.
WO2014085607A1 Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.
EP1632493A1 Dihydropteridine derivatives, methods for their preparation and their use as drugs Dihydropteridinone derivatives (I) are new. Dihydropteridinone derivatives of formula (I) and their tautomers, isomers, acid addition salts, solvates and hydrates are new. L = a bond, A, OA or N(R7>)A; A = 1-6C alkylene, 2-6C alkenylene, 2-6C alkynylene, 3-7C cycloalkylene, (1-4C)alkylene(6-10C)arylene(1-4C)alkylene or (1-4C)alkylene(6-10C)arylene, all optionally substituted with R9>; R1>, R2> = H or 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl, all optionally substituted with R9>, or R1>+R2> = 2-6C alkylene with 0-2 CH2 groups replaced by O or NR7>, optionally substituted with R9>; R3> = H or 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-8C cycloalkyl or 6-14C aryl, all optionally substituted with R9>; or R3>+R2> or R3>+R1> = 2-6C alkylene optionally substituted with R9>; R4> = H, halo, CN, OH, NR7>R8>, A' or OA'; A' = 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl, all optionally substituted with R10>; R5> = phenyl optionally substituted with R11>; phenyl monosubstituted with R6>; or 1-4C alkyl optionally substituted with R9>; R6> = NR7>R8> or 5- to 10-membered heterocycloalkyl with 1-3 heteroatoms (N, O, S), optionally substituted with R12>; R7>, R8> = H or 1-6C alkyl; R9> = halo, 1-4C alkyl, 1-4C alkoxy, CN, OH or CF3; R10> = halo, OH, oxo, 1-6C alkoxy, COOR7>, NR7>R8>, CONR7>R8>, SO2R7>, CHF2 or CF3; R11> = halo, OH, CN, 1-4C alkyl, 1-4C alkoxy, COOR7>, NR7>R8>, CONR7>R8>, SO2R7>, CHF2, CF3, 6-10C aryl or (6-10C)aryl(1-6C)alkyl; and R12> = halo, CF3, 1-6C alkyl, (6-10C)aryl(1-6C)alkyl 3-8C cycloalkyl or (3-8C)cycloalkyl(1-6C)alkyl. Independent claims are also included for intermediates of formula (A8), (A7a), (A7b) and (A5). PG = protecting group. [Image] [Image] [Image] - ACTIVITY : Virucide; Anti-HIV; Antiinflammatory; Immunosuppressive; Antibacterial; Fungicide; Antiparasitic; Cytostatic; Dermatological; Antipsoriatic; Osteopathic; Vasotropic; Cardiant. Compounds (I) have good to very good activity in a HeLa S3 cytotoxicity assay, e.g. with an EC50 of less than 5 mu M, generally less than 1 mu M. - MECHANISM OF ACTION : Polo-like kinase inhibitor.
CN101953889A Compound ceftiofur suspension emulsion injection and preparation method thereof The invention discloses a compound ceftiofur suspension emulsion injection, which comprises the following components in percentage by mass: 1.5 to 15 percent of ceftiofur hydrochloride, 1.5 to 15 percent of magnolia flower oil, 1 to 10 percent of surfactant, 3 to 30 percent of oil for injection, 0.1 to 1 percent of antioxidant, 0.01 to 0.1 percent of thickening agent, and the balance of water for injection, wherein the sum of the mass percents of the components is 100 percent. The compound ceftiofur suspension emulsion injection has simple operation for the preparation method, strong antibacterial property and lasting pharmacological effect, and avoids stresses caused by multi-time administration of conventional formulations to animals; furthermore, the preparation cost is much lower than that of an oil suspension, and the compound ceftiofur suspension emulsion injection has a very high popularization and application value.
CN1682693A In site gel medicine transfer system for hardening treating angioma and vascular deformity The medicine transfer system for hardening treatment of angioma and vascular deformation has in-site gel as medicine transfer system for injection to tumor cavity. The medicine transfer system may contain no any medicine; the angioma may be angioma or lymphangioma; the vascular deformation includes venule deformation, vein deformation, arteriovenous deformation, lymphatic vessel deformation and mixed deformation; and the medicine includes various kinds of medicine injected into tumor to cause angioma atrophy and elimination, such as sodium morrhuate, alum, Pingyangmycin, etc. The delayed releasing in-site gel can prolong the action time of medicine, reduce medicine amount, raised hardening effect and medicine bioavailability and reduced medicine toxicity.
WO2008084962A1 THIAZOLE COMPOUND (AS PPARδ) LIGAND AND PHARMACEUTICAL, COSMETIC AND HEALTH FOOD COMPRISED THEREOF The present invention relates to a thiazole compound as a peroxisome proliferator activated receptor δ (PPARδ) activator or pharmaceutically acceptable salts thereof, and a pharmaceutical composition, a functional cosmetic composition, a health food, health beverages, a food additive and animal feeds containing the same.
US20090105197 Use of Sodium Channel Blocking Compounds and Aspirin in Manufacturing Drugs for Producing Analgesia Synergistically in Mammals This invention relates to the use of combinations of a sodium channel blocking compound that binds to an SSI or SS2 site of extracellular region of a sodium channel alpha subunit, and aspirin in manufacturing drugs for producing synergistically analgesic effect in mammals. Pharmaceutical compositions based upon this invention can enhance analgesic effect and reduce dosage of aspirin, therefore side effects and adverse reactions are decreased accordingly.
CN1903197A Nizatidine dispersion tablets A dispersing tablet of nizatitine is prepared proportionally from nizatidine, diluent, disintegrant, lubricant and adhesive.
CN102816107A Carbazole derivative and preparation method and use thereof The invention provides a carbazole derivative, which has excellent activity for inhibition of cholinesterase. The invention also provides a preparation method of the compound and application thereof in preparation of drugs for treatment of neurodegenerative diseases. The structural formula of the compound is as follows.
US20120071406 Modified vegf-a with improved angiogenic properties The present invention is directed to methods and compositions for making and using chimeric polypeptides that comprise a VEGFR-2 ligand. The chimeric molecules of the present invention retain VEGFR-2 binding activity and an enhanced angiogenic activity as compared to native VEGF-A.
EP1495016A2 Heterocyclic compounds and their use as modulators of p38 map kinase The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a p38 MAP kinase such as rheumatoid arthritis and osteoarthritis; the compound being of the general formula (I): wherein U, T, V and W are each a nitrogen atom or a group CR4 provided that no more than three of U, T, V and W are nitrogen atoms; R0 is hydrogen, C1-4 hydrocarbyl, halogen or a group -A-R3; R1 is hydrogen, C1-4 hydrocarbyl or a group -A-R3; provided that only one of R0 and R1 is a group -A-R3; R2 is hydrogen, C1-4 hydrocarbyl or halogen; A is a carbon- or heteroatom-containing linker group having a linking chain length of one or two atoms; R3 is a monocyclic or bicyclic heteroaryl group containing from five to twelve ring members; each group R4 is independently selected from hydrogen, hydroxy, halogen, nitro, cyano, a monocyclic heterocyclic group having up to seven ring members, a group N(R5)2, a group C(O)N(R6)2, a group S02N(R6)2, a group Ra-Rb and a group Y; provided that no more than one group Y is present;
WO2012045894A1 Compounds and compositions for the treatment of illnesses caused by the hepatitis b virus The invention relates to agents able to inhibit the expression of hepatitis B virus genes by inhibiting the maturation of the various RNAm of said virus using U1 RNAs, by means of interferent RNAs or synergistic combinations that include both inhibiting agents. The invention also relates to the use of said agents and to compositions for the treatment of illnesses caused by a Hepatitis B virus infection.
US20080312337 Anticancer Composition Comprising Obovatol or Obovatal Disclosed herein is an anticancer composition, comprising obovatol, represented by the following Chemical Formula 1, obovatal, represented by the following Chemical Formula 2, and/or pharmaceutical salts thereof. The composition exhibits the activity of inhibiting the growth of cancer cells and suppressing the expression and activity of matrix metalloproteinases (MMPs), and thus can be useful for the prophylaxis and treatment of cancer as well as for the inhibition of cancer metastasis.
EP0841937B2 Use of betaglycan to reduce scarring The present invention concerns soluble betaglycan for use in promoting the healing of wounds or fibrotic disorders with reduced scarring, together with methods for same.
US20120201857 Transdermal delivery system for therapeutics The present invention provides a method and product for transdermal delivery of therapeutics, including neurotoxins and methods for use thereof. The method and system comprises pharmaceutical compositions for facilitating transdermal delivery of therapeutics without pain by absorption and more particularly a series of pharmaceutical formulations for topical administration of neurotoxins to humans, including a neurotoxin, such as a botulinum toxin, and absorption enhancing agents that facilitate absorption of the neurotoxin through the skin of the patient and do not eliminate the bioactivity associated with the neurotoxin. The pharmaceutical compositions are topically applied on a patient, and are generally in a cream or gel form.
US20080131524 Compositions for treatment of viral-induced skin lesions and methods of using same A composition and method for treatment of viral-induced skin lesions, such as warts, are described. The composition is comprised of tea tree oil and/or derivatives from tea tree oil and one or more minerals, such as iodide and/or selenium. The composition is used to prepare medicaments for the treatment of viral-induced lesions, such as warts caused by the Molluscum contagiosum virus, human papillomavirus, and/or herpes simplex virus. The composition is applied topically to the human epidermis and/or to the genital tract as needed.
US7098337 Serotonin receptor agonists such as 6-chloro-4-methyl-1,2,3,4 -tetrahydro-2,4a,5-triaza-fluorene, used for prophylaxis of nervous system, cardiovascular, gastrointestinal, eating or sleep disorders, and as antidiabetic agents The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.
US20110190380 Methods for delivery of sirna to bone marrow cells and uses thereof The present invention relates to a method for the delivery of therapeutic oligonucleotides to bone marrow, and in particular delivery of siRNA to a subset of bone marrow cells. The method comprises systemically administering siRNA to a subject in need thereof, to reduce or inhibit expression of a gene associated with a disease or disorder or to symptoms associated with a disease or disorder associated with the cells. The invention further relates to chemically modified siRNA compounds, to pharmaceutical compositions comprising such compounds and to methods of using such compounds and compositions in the treatment of disease.
WO2010102281A3 Inhibitors of anaphase promoting complex activity The invention provides an anti-proliferative composition comprising a non-peptide analog of the C-terminal isoleucine-arginine (IR) tail motif of an activator of an anaphase promoting complex (APC). The invention further provides methods of inhibing the ubiquitination activity of the APC by administering compositions of the invention.
CN101389606A Pyridinyl amine derivatives as inhibitors of cholesteryl ester transfer protein (CETP) The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the variables are as defined, useful as inhibitors of chlosteryl ester transfer protein.
WO2003092720A8 A combination product comprising an anti-coagulant and anti-arrhythmic oxabispidenes There is provided a combination product comprising: (1) an anti-coagulant; and (1) a compound as defined in claim 1 of WO 01/28992 or (2) a compound of Claim 34 of WO 01/28992 or (3) Compound A or B or C or D (or pharmaceutically-acceptable salts thereof) for use in treating arrhythmia or a coagulation controlled complication thereof.
US7342024 4-Oxo-1-3-substituted phenyl-1,4-dihydro-1,8-naphthyridine-3-carboxamide phosphodiesterase-4 inhibitors Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation and useful for the enhancement of cognition
US7592360 3-fluoro-piperidines as NMDA/NR2B antagonists Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for treating conditions such as, for example, Parkinson's disease, Alzheimer's disease, migraine, epilepsy and pain.
EP1251874B1 Stabilised pharmaceutical compositions and process for their preparation comprising an antibiotic and an expectorant Compositions for the prophylactic or therapeutic treatment of bacterial diseases in humans and animals, comprising as essential active ingredients a quinolone- or naphtyridone-type antibiotic or an active chemical derivative thereof and an expectorant, glacial acetic acid, water and a stabilizing agent. The compositions are stable upon storage over a broad range of temperature. The invention concerns also the combined use of a quinolone- or naphtyridone-type antibiotic or an active chemical derivative thereof and an expectorant for the treatment of bacterial infections in humans and animals, and a process for the preparation of the aforementioned compositions.
CN102579352A Clarithromycin freeze-dried liposome and preparation method thereof The invention discloses a clarithromycin freeze-dried liposome which is prepared by carrying out freeze-drying after mixing liposome solution and a cryoprotectant. 5 g to 20 g of cryoprotectant is added into each 100 mL of the liposome solution; 100 ml of the liposome solution is prepared from the following raw materials: 0.05 g to 2.0 g of clarithromycin, 0.01 g to 2.0 g of sterol substance, 0.2g to 10g of phospholipid, 0.01 g to 1.0 g of fatty acid and the balance of phosphate buffered solution; and the cryoprotectant is formed by one or more of cane sugar, glucose, trehalose, maltose and mannitol. The invention further discloses a preparation method of the liposome. The clarithromycin freeze-dried liposome disclosed by the invention can be used for obviously reducing the pain of the administration sites and the vascular irritation which are caused by clarithromycin, various indexes of the clarithromycin freeze-dried liposome all meet the requirement on research and development of new drug by the State Food and Drug Administration, and the foundation is laid for the industrial production and the clinical application of aclarithromycin liposome preparation.
CN1593408A Alkaloids sophora flavescen pellicle and its preparation process Disclosed is a alkaloids sophora flavescen pellicle and its preparation process, wherein the pellicle comprises matrine and oxymatrine as the active constituents, and added anti-oxidant and fill forming material. The preparation process includes, steeping the film forming material with water, dissolving by water-bath, dissolving the matrine and total matrines with the mixed solution of water and ethanol, mixing with the aqueous solution of the film forming material, adding anti-oxidant simultaneously, mixing, removing air bubbles, coating into film and drying.
WO2007144530A3 Free-radical-scavenger cosmetic composition The invention relates to a free-radical-scavenger cosmetic composition. This composition is characterized in that it comprises a combination of at least three of the following free-radical-scavenger active substances; said combination comprising: 1) either ebselen; or idebenone; or a combination of the two; and 2) at least one free-radical-scavenger active substance, or at least two free-radical-scavenger active substances, so as to obtain said combination of at least three free-radical-scavenger active substances, chosen from the group consisting of: a) a substance having the following chemical formula (I) in which: R = a linear or branched, saturated or unsaturated C1-C16 hydrocarbon-based chain; R1, R2 and R3 are identical or different, and represent a hydrogen atom, or a methyl radical or a methoxy radical or its esters; b) an extract of Edelweiss; c) an extract of Emblica; d) N-acetylcysteine. The free-radical scavenger activity is greatly improved with the invention.
CN101732307A Medical use of guaifenesin The invention relates to the use of guaifenesin in the preparation of medicaments for preventing and treating cardiovascular and cerebrovascular diseases and tumors. Experiments prove that the guaifenesin has remarkable effects of preventing and curing angina, myocardial infarction, cerebral hemorrhage, cerebral thrombosis and digestive system neoplasms and the like. At the same time, the invention also provides the use of the guaifenesin in the preparation of medicinal preparations for preventing and treating cardiovascular and cerebrovascular diseases and tumors.
CN102949382A Dextrorotatory ketoprofen composition and preparation method thereof The invention relates to the technical field of medicine, and provides a dextrorotatory ketoprofen composition and a preparation method thereof, and especially a dextrorotatory ketoprofen preparation for external use and a preparation method thereof; the composition of the invention has better curative effect and less side effect than dextrorotatory ketoprofen oral preparations.
US20120328526 Modulation of Nad+ Activity in Neuropathophysiological Conditions and Uses Thereof The present invention provides a method of treating a mammal having a neuropathophysiological condition, comprising the step of administering to the mammal in need of such treatment a compound selected from nicotinamide or salts or prodrugs thereof, nicotinamide mononucleotide or salts or prodrugs thereof, nicotinamide adenine dinucleotide or salts or prodrugs thereof, nicotinamide riboside nicotinamide or salts or prodrugs thereof, phosphoribosyltransferase, or combinations thereof. Further provided is a method for treating a mammal having a neuropathophysiological condition or suspected to develop said neuropathophysiological condition, comprising the step of administering to said mammal an inhibitor of CD38 NAD+ glycohydrolase activity.
US20120077809 Pyrimidopyridazine derivatives useful as p38 mapk inhibitors A compound formula (IA) or (IB), or a pharmaceutically acceptable thereof; wherein the substituents are defined as in the claims, and their use as P38 MAP kinase.
US20050038108 4S, 5R, 6R)-5-Acetylamino-4-azido-6-[(S)-4-nitrophenoxycarbonyloxy)-(2-oxo-[1,3]dioxolan-4R-yl)methyl]- 5,6-dihydro-4H-pyran2-carboxylic acid methylester; modified at the carboxyl or hydroxyl or amino functions; orthomyxovirus and paramyxovirus infections; a long lung residency time and high potency The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, SO2NH, NHCO or NHCONH; m is either 0 or 1; n is an integer from 2 to 6; q is an integer from 0 to 3; and Y is hydrogen or an aromatic substituent, or a pharmaceutically acceptable derivative thereof; methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection.
CA2430814C A process for the preparation of paclitaxel A process for the preparation of paclitaxel starting from 10-deacetylbaccatine III.
CN102784110A Oxaprozin nanosphere and preparation method thereof The invention discloses a preparation method for an oxaprozin nanosphere. The preparation method is characterized in that the oxaprozin nanosphere is prepared by high frequency ultrasonic technology, the encapsulating rate reaches to above 90%, the grain size reaches to 80-130nm, simultaneously a capsule wall material, an emulsifying agent and a thickening agent are preferably selected, the digestion performance of products is improved, the stability of products is increased, the curative effect of products is improved, and a promising effect is obtained.
CN102028911A External medicament for treating tinea pedis The invention discloses an external medicament for treating tinea pedis. The medicament consists of the following components by weight: 15 to 40g of golden thread, 5 to 20g of lightyellow sophora root, 5 to 15g of amur corktree bark, 10 to 45g of chinaberry bark and root-bark, 10 to 20g of liquoric root, 5 to 20g of cnidium monnieri, 5 to 25g of zedoary, 10 to 30g of sandalwood, 5 to 15g of borneol, 5 to 20g of gardenia, 5 to 15g of Mongolian dandelion herb, 1 to 2.5g of vitamin B1 and 100 to 500g of vaseline. The preparation method of the medicament comprises the following steps of: blending the golden thread, the lightyellow sophora root, the amur corktree bark, the chinaberry bark and root-bark, the liquoric root, the cnidium monnieri, the zedoary, the sandalwood, the gardenia and the Mongolian dandelion herb, selecting, cleaning, drying, baking and crushing the materials, and sterilizing the powder at a high temperature; blending the borneol and the vitamin B1 in proportion, crushing the mixture into fine powder, and screening the powder with a 200-mesh sieve; and blending the two kinds of medicinal powder and the vaseline, and uniformly stirring to obtain a pasty ointment.
US20080312191 Novel Urokinase Inhibitors The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to the use of said uPA inhibitor compounds as a medicament and the use of said uPA inhibitor compounds for the preparation of a medicament for the treatment of conditions chosen from the group comprising cancer, tumour growth, tumour invasion, tumour metastasis, diabetic retinopathy, hemorrhagic atherosclerosis and inflammatory conditions, such as rheumatoid arthritis and psoriasis.
CA2217767C Low ph skin-treatment composition A low pH skin-treatment composition employs cationic surfactants generally known to be skin irritants and a fatty acid, together with a hydrocarbon component in an oil-in-water emulsion. The addition of fatty acid to the cationic surfactant appears to form a complex which prevents the cationic surfactant from irritating the skin and at the same time substantially reduces pH of the composition. The resulting composition is not skin irritating, and reflects a pH of about 2-4. The composition may be used to restore pH of skin after exposure to alkaline compositions, and as a vehicle for the administration of active agents having an acidic pH.
WO2009028650A1 Emulsion-type external preparation, and method for production thereof Disclosed are: an emulsion-type external preparation in which the precipitation of crystals of an alkali metal salt or an alkali earth metal salt of a carboxylic acid-type pharmaceutical active ingredient compound or a hydrate of the salt can be prevented effectively, which is mildly irritative, and in which the decrease in the content of the active ingredient can be prevented; and a method for producing the emulsion-type external preparation. Specifically disclosed are: an emulsion-type external preparation produced by mixing an emulsion and a treated acidic water-soluble polymer solution, wherein the emulsion is produced by emulsifying thefollowing components (a) and (b): (a) an aqueous phase comprising a pharmaceutical active ingredient compound having a carboxylate group and taking the form of an alkali metal salt or an alkali earth metal salt and an aqueous solvent; and (b) an oily phase comprising at least one oily component selected from the group consisting of a fatty acid ester, a hydrocarbon, an animal or plant oil, a hydrogenated oil thereof and a natural wax, and wherein the treated acidic water-soluble polymer solution is prepared by treating the whole or a part of an acidic water-soluble polymer with a basic substance in an aqueous solvent; and a method for producing the emulsion-type external preparation. Also specifically disclosed are: an emulsion-type external preparation produced by mixing an emulsified composition comprising a pharmaceutical active ingredient compound having a carboxylate group and taking the form of an alkali metal salt or an alkali earth metal salt with a solution comprising an acidic water-soluble polymer treated with a basic substance; and a method for producing the emulsion-type external preparation.
US6958238 Isolated dishevelled associated kinases, polynucleotides encoding the kinases, and methods of use thereof The invention provides Dishevelled Associated Kinase polypeptides, which phosphorylate Dsh proteins involved in the Wnt/Wg signalling pathway. Isolated polynucleotides encoding DAK polypeptides are further provided, as are recombinant vectors, and host cells comprising the polynucleotides. Methods of using the polynucleotides and polypeptides of the invention are further aspects of the invention, including assays to detect agents which modulate DAK kinase activity. Further provided are methods of modulating pathways involved in control of cell proliferation.
EP2515845A1 Dry powder combination of tiotropium, formoterol and a cromoglicic acid derivative The present invention relates to a pharmaceutical composition wherein tiotropium combined with formoterol which is a ß-2 adrenergic receptor antagonist and an effective amount of a cromolyn derivative are formulated together and are used for the treatment of respiratory disorders by inhalation route.
CN101829094A Application of ring E bromine substituted silybin in preparing medicaments for treating viral hepatitis B The invention relates to application of ring E bromine substituted silybin in preparing medicaments for treating viral hepatitis B, in particular to application of a compound of a formula (1) and a pharmaceutically acceptable salt thereof in preparing medicaments for clearing away hepatitis B surface antigens (HBsAg) and hepatitis e antigens (HBeAg) and suppressing the HBV (Hepatitis B Virus) DNA replication. The compound has definite activity on suppressing the HBsAg and the HBeAg, and in the presence of a concentration of 100 micrograms/milliliter, the intensities of the compound for clearing away the HBsAg and the HBeAg are respectively 38.2 percent and 39.1 percent which are respectively 2.4 times and 2.3 times of that of a positive control medicament (10,000 units/milliliter of alpha-interferon). Meanwhile, in the presence of the concentration, the suppression ratio of the compound on the HBV DNA is 36 percent which is close to that of the alpha-interferon. Accordingly, the flavone lignan or the pharmaceutically acceptable salt thereof are indicated to be capable of being used for preparing non-nucleoside medicaments for clearing away the HBsAg and the HBeAg, suppressing the HBV DNA replication and treating HBV infection diseases.
CN102731385A 3-chloro-N-methyl-2-picolinamide compound and 3-methoxyl-N-methyl-2-picolinamide compound and use thereof as anticancer medicament The invention relates to a 3-chloro-N-methyl-2-picolinamide compound and a 3-methoxyl-N-methyl-2-picolinamide compound and use thereof as anticancer medicament. The invention provides a compound of formula I or a pharmaceutically acceptable salt thereof, the compound and the pharmaceutically acceptable salt inhibiting VEGER-2 and other kinases, and the use thereof in preparing a medicament for treating a disease mediated by the VEGER-2 and other kinases, wherein, A is selected from chlorine or methoxyl; R1, R2 and R3 are selected from the group consisting of a halogen, a cyano, a hydroxyl, a trifluoromethyl, a methoxyl, a trifluoromethoxyl, a substituted or unsubstituted C1-C6 straight chain, a C1-C6 branched alkyl, a C6-C10 cycloalkyl, a C6-C10 aryl, a C6-C10 heteroaryl, or a C6-C10 heterocyclyl containing one or more atoms selected from N, S and O. The substituent is selected from the group consisting of an amino, a halogen, a C1-C6 alkyl, a hydroxyl, a C1-C6 alkoxy, a nitro, a cyano, a mercapto, a C1-C6 alkylthio, a halogen-C1-C6-alkylthio, a heterocyclyl, a heteroaryl, heterocyclylalkyl, a heteroaryl C1-C6 alkyl, a C1-C6 alkanoyl or a carbamoyl.
WO2009132979A1 4-trimethylammonio-butyrates as cpt2 inhibitors This invention relates to novel 4-trimethylammoniobutyrates of the formula wherein A1, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.
CN101744820A Medicine composite containing dextromethorphan hydrobromide The invention provides a medicine composite containing dextromethorphan hydrobromide, which contains cyclodextrin, the weight of which is 5-20 times that of the dextromethorphan hydrobromide, wherein the cyclodextrin is beta-cyclodextrin. The oral dextromethorphan hydrobromide composite can quickly relieve a cough with quick effect, good absorption, high absorptivity of above 98%, no bitter taste and good mouthfeel.
CN1732931A Antibacterial compound drug of sulbenicillin sodium for injection The invention provides an antibacterial composition of sulbenicillin sodium for injection, which comprises sulbenicillin sodium and sulbactam sodium by the weight ratio of 1-32:1. The antibacterial compound preparation has substantial synergy actions, and can effectively inhibit the reactivity of beta-lactamase.
US20090074691 Topical Delivery System for Antiaging and Skin Whitening Agents This invention relates to certain hydroxyaryl alkanols, alkyl amines, alkyl amino acids, alkyl amino esters, and alkyl amino alkanols (“Hydroxyaryl compounds”) of formula (I). A method of topical application of said hydroxyaryl compounds is also disclosed. The treatment of certain enzyme dysfunctions that cause skin or hair condition such as darkened skin including age spots, dark circles around the eyes, and discoloration of skin from stretch marks; skin conditions related to acne including excess facial oil and facial pore size; premature hair aging including hair loss and graying; inflammation including intra-cellular and extra-cellular inflammation; skin aging including wrinkles and fine lines; loss of collagen including thinning skin and loss of skin pliability; malfunction of tyrosinase group of enzymes; and malfunction of matrix metalloprotease group of enzymes with said hydroxyaryl compounds is also disclosed:
US20100190752 tapentadol and antiepileptic such as gabapentin; synergistic pain relief A composition of matter comprising in combination as component (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and as component (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said composition of matter, and a method of treating pain, e.g. neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.
WO2006056823A1 Modulating retinal pigmented epithelium permeation by inhibiting or activating vegfr-1 The present invention relates to the use of an agonist or an antagonist of VEGFR-1 in the treatment or prevention of diseases wherein disorders of the retinal pigment epithelium permeation are involved.
EP1556414B1 Heparin-derived oligosaccharide mixtures, preparation thereof and pharmaceutical compositions containing the same The invention concerns heparin-derived polysaccharide mixtures having an average molecular weight of 1500 to 3000 daltons and an anti-Xa/anti-IIa ratio higher than 30, their preparation method and pharmaceutical compositions containing same.
CN101296701A A combination of compounds, which can be used in the treatment of respiratory diseases, especially chronic obstructive pulmonary disease (COPD) and asthma The present invention provides pharmaceutical compositions comprising a glucocorticosteroid and a compound of formula: wherein m, R<1>, R<2>, R<3>, and R<4> are as defined in the specification, and their use in therapy.
EP2740727A1 Quinazolinone analogues for use as anticonvulsant agents The present invention relates to a compound according to formula 1: wherein each R1 is independently selected from the group consisting of chloro, methoxy, aryl, preferably phenyl or naphthyl, heteroaryl, preferably furyl, pyrrolyl, thienyl, imidazolyl, thiadiazolyl, pyridinyl, pyridazinyl, pyrimidinyl, benzothiazolyl and oxadiazolyl, mercapto and alkylthio, most preferably is chloro or methoxy; R2 is selected from hydrogen or -CO-(CH2)m-R3; R3 is selected from the group consisting of alkyl, alkoxyl, aryl, or heteroaryl ring system, preferably furyl, pyrrolyl, thienyl, imidazolyl, thiadiazolyl, pyridinyl, pyridazinyl, pyrimidinyl, benzothiazolyl or oxadiazolyl; o is an integer from 1-4; n and m are independently selected integers form 0-10, preferably from 0-5, as well as to a method for its preparation, pharmaceutical compositions comprising said compound as well as said compound and said pharmaceutical composition for use in treatment of convulsion and/or epilepsy.
CN103720884A Costus root health care wine for infertility The invention relates to a costus root health care wine for infertility. The wine is prepared by the following steps: grinding 25g of costus root, 11 g of black alum, 16 g of processed santal, 19 g of prepared rhizome of rehmannia, 15 g of frankincense and 21 g of root bark of the peony tree into a coarse powder; adding the above medicine and 3000 g of red wine into a jar and soaking for 1-3 months; pumping the soaked wine with a liquor pump, filtering with a filter cloth of 50-60 mesh, and quantitatively filling the filtrate to obtain the costus root health care wine for infertility. The costus root health care wine for infertility has the advantages of simple production method, convenience for drinking, and effects of warming kidney, invigorating spleen, nourishing blood and regulating menstruation, and can help women warm the kidney, strengthening the spleen, nourish blood, regulate menstruation and alleviate infertility symptoms by long-term drinking.
US20100016221 Method of degrading protein by chaperone-mediated autophagy The present invention provides a method of degrading a target protein in a subject comprising administrating to the subject an effective amount of any of: (a) a peptide comprising an HSC70-binding moiety and a target protein-binding moiety; and/or (b) a polynucleotide encoding the peptide of (a). The present invention further provides an isolated peptide comprising an HSC70-binding moiety and a target protein-binding moiety, an isolated polynucleotide encoding said peptide, and an expression vector comprising said polynucleotide.
US20100292211 Antipsychotic treatment based on snp genotype The present invention relates to the prediction of antipsychotic treatment efficacy based on a patient's genotype at one or more single nucleotide polymorphism (SNP) loci and to the treatment of a patient based on such prediction.
US20080118558 2-Isopropyl-5-methyl-cyclohexanecarboxylic acid [2'-hydroxy-2'-(3''-hydroxy-phenyl)-ethyl]-N-methyl-amide; topical analgesics and antipruritic and antitussive agents for disorders caused by kidney failure or cholestatic jaundice N-(Substituted-aryl-hydroxyalkylidene)-cycloalkyl carboxamide compositions are disclosed that target molecular elements on sensory nerves. These compounds, preferably administered topically, inhibit the perception of itch and pain and have prolonged duration of action.
WO2005116023A8 3- {4- (pyridin-3-yl) phenyl} -5- (1h-1, 2, 3-triazol-1-ylmethyl) -1, 3-oxazolidin-2-ones as antibacterial agents Compounds of formula (I), as well as pharmaceutically-acceptable salts and pro-drugs thereof, are disclosed wherein R1, R2, R3, and R4 are defined herein. Also disclosed are processes for making compounds of formula (I) as well as methods of using compounds of formula (I) for treating bacterial infections.
US20120027815 Use of plasma membrane calcium atpase (pmca) inhibitors to inhibit sperm mobility The invention relates to the use of plasma membrane calcium ATPase (PMCA) inhibitors for inhibiting sperm mobility to achieve a contraceptive effect. The invention further relates to contraceptive agents comprising one or more PMCA inhibitors.
WO2005106473A1 Method of screening therapeutic agent for neurodegenerative disease A method of screening a substance capable of inhibiting any binding between protein with S-100β binding capacity and S-100β, comprising bringing a protein with S-100β binding capacity into contact with S-100β in the presence and absence of an analyte, measuring the levels of binding between protein with S-100β binding capacity and S-100β in two instances, and comparing them to each other. The substance obtained by this screening method, partial peptide from the protein of the invention, antibody capable of inhibiting any binding between the protein and S-100β and polynucleotide comprising the base sequence, or part thereof, complementary to the polynucleotide coding for the protein are useful in the treatment and diagnosis of, for example, neurodegenerative diseases, such as Alzheimer's Disease, Parkinson's disease and amyotrophic lateral sclerosis.
CN103463496A Drug for treating ankylosing spondylitis The invention relates to a drug for treating ankylosing spondylitis. The drug is prepared from the following substances in proportion by weight: dysosma difformis, seeds of Chinese dodder, amethyst, exocarpium, abalone, litchi, exocarpium benincasae, spina gleditsiae, polygonum orientale, stalactite, humifuse euphorbia herb, glechoma longituba, common alstonia bark leaves, herba selaginellae, pepperweed seeds, saururus chinensis, chingma abutilon seeds, caulis bambusae in taeniam, murraya paniculata, folium turpiniae, peucedanum decursivum maxim, Chinese honey locust, grand torreya seeds, folium polygoni tinctorii, veronicastrum herbs, ophicalcitym, Chinese holly, coxcomb, eucommia ulmoides, green frontiers stones, milfoil, nodular branches of pine, balsamine, soybean germinated, radix ampelopsis, desert asparagus, lysionotius pauciflorus maxim, tuber fleeceflower stems, leaves of paniculate microcosm, radix scrophulariae, akebia trifoliata koidz, longan pulp, wild buckwheat rhizome, gordon euryale seeds, dayflowers, Chinese starjasmine stems, valeriana jatamansi jones, fructus piperis longi, string beans and corn stigmas. The drug for treating ankylosing spondylitis disclosed by the invention is prepared from natural medicines, has a clear curative effect, can be used for effectively treating the ankylosing spondylitis, and therefore, the drug is very suitable for clinical application.
CN101797334A External ointment for treating onychomycosis and paronychia The invention relates to an external ointment for treating onychomycosis and paronychia, which is characterized by comprising the following components by weight ratio: 15 of croton, 15 of rehmannia, 15 of angelica, 30 of salvia miltiorrhiza, 10 of cicada slough, 15 of radix sophorae falvescentis, 15 of Cortex dictamni, 6 of licorice, 15 of radix scutellariae, 30 of Rhizoma smilacis Glabrae, 10 of borneol, 2 of miconazole nitrate, 9 of octodecyl alcohol, 6 of cetanol, 10 of glycerin monostearate, 205 of tween, 18 of glycerol, 1 of sodium benzoate and 55 of purified water. The invention for treating onychomycosis and paronychia has short duration of treatment, high curative effect and low recurrence rate.
US20110046172 Medicinal Compositions A composition, in parenteral unit dosage form or in a unit dosage form suitable for delivery via the dermis or mucosa, comprises buprenorphine and an amount of naloxone such that the ratio by weight of buprenorphine to naloxone delivered to or reaching the plasma of a patient is in the range of from 7.5:1 to 12.4:1. The analgesic action of the buprenorphine is potentiated by the low dose of naloxone, which also serves to reduce the likelihood of abuse of the composition by drug addicts. Also provided are a method of treatment of pain and the use of naloxone and buprenorphine for the manufacture of a medicament.
US20090082432 Deuterium-enriched ramelteon The present application describes deuterium-enriched ramelteon, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US7736666 Consists of naproxen, a butyl spacer and a nitrogen oxide (NO)-releasing nitrate group, linked together into a single molecule; useful as antiinflammatory agent and an analgesic The present invention claims and discloses a pharmaceutical composition suitable for oral administration, in form of an emulsion pre-concentrate, comprising (i) a compound of formula (I); (ii) one or more surfactants; (iii) optionally an oil or semi-solid fat; said composition forming an in-situ oil-in-water emulsion upon contact with aqueous media such as gastrointestinal fluids. The composition may optionally also comprise one or more short-chain alcohols. The pharmaceutical composition is useful in the treatment of pain and inflammation.
CN101560178B Polysubstituted indoline compound, preparation method and medical application thereof The invention provides a polysubstituted indoline compound with structural formula shown in general formula I, pharmaceutically acceptable pharmaceutical acid addition salt thereof or pharmaceuticallyacceptable hydrate of pharmaceutical acid addition salt. The invention also provides a preparation method of the above compound. In addition, the invention also provides applications of the above compound in treating benign prostatic hyperplasia and cardiovascular disorders and in adjusting intraocular pressure.
WO2012158866A9 Treatment of autoimmune disorders and infections using antagonists of sgk1 activity The present invention provides novel methods for treating Th2-mediated immune disorders and enhancing Th1-mediated immune responses in a subject comprising administering to the subject, a pharmaceutical composition comprising a serum-glucocorticoid regulated kinase 1 (SGK1) inhibitor and a pharmaceutically acceptable carrier. Methods for treating a wide range of autoimmune diseases are also taught. The present invention also provides methods for augmenting the treatment of subjects having viral or parasitic infections, or which have cancerous tumors.
US20110293681 Hand sanitizing patch having an integrally bonded antimicrobial The present invention provides for topical adhesive patch that includes a backing having a front side and a back side; a formulation in contact with the front side of the backing, the formulation including an adhesive; and at least one antimicrobial. The antimicrobial is integrally bonded to the back side of the backing. The present invention also provides for a method of reducing the number of microbes located upon a topical skin surface of a mammal, as well as a method of preventing the transmission of a communicable disease capable of being transmitted by physical contact. The methods include topically contacting a skin surface of the mammal with the back side of the topical adhesive patch.
EP2526091A1 Derivatives of pyridoxine for inhibiting hiv integrase The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or compositions thereof wherein X, Y, R1-R5 are defined in the specification. Compounds of Formula I inhibit HIV-integrase enzyme and are useful for preventing and treating of HIV infection, AIDS or AIDS-related complex (ARC), and other diseases and conditions caused or mediated by HIV infection.
CN102351857A Tropiseiron hydrochloride compound The invention belongs to the technical field of medicines, and particularly relates to a tropiseiron hydrochloride compound and a preparation method thereof. The invention also relates to application of an injection containing the tropiseiron hydrochloride compound in preparation of drugs for treating nausea and vomit.
EP1727543B1 Use of 14,15-dihydro-20,21-dinoreburnamenin-14-ol for the treatment and/or prevention of serious depression The invention relates to a novel therapeutic use of 14,15-dihydro-20,21-dinoreburnamenin-14-ol for the treatment of serious depression in humans, particularly for the treatment of patients resistant to conventional anti-depressant treatments and for treatment of sleep/waking cycle disorders.
WO2009119601A1 Water-based adhesive skin patch comprising ketoprofen lysine salt Disclosed is a water-based adhesive skin patch comprising ketoprofen, which is improved in the efficiency of production work and has excellent storage stability and transdermal absorption properties of ketoprofen contained therein. Specifically disclosed is a water-based adhesive skin patch containing ketoprofen lysine salt, which comprises a support and an adhesive agent (paste) layer laminated on the support. The adhesive skin patch is characterized in that ketoprofen lysine salt (the main ingredient) is contained in a paste in a completely dissolved state, wherein the paste does not contain glycerin and contains a polyethylene glycol having an average molecular weight of 1000 or less. In the adhesive skin patch, the polyethylene glycol having an average molecular weight of 1000 or less is one or more types of polyethylene glycol selected from the group consisting of polyethylene glycol 200, polyethylene glycol 400, polyethylene glycol 600 and polyethylene glycol 1000.
WO2006125121A2 Antimicrobial composition comprising a cationic surfacant and an iodinated sulpone compound An antimicrobial composition comprising (a) a cationic surfactant derived from the condensation of fatty acids and esterified dibasic amino acids, such as lauric arginate, and (b) an iodinated sulfone compound such as diiodomethyl-p-tolylsulfone. The composition may be used as a stand-alone antimicrobial formulation, or in combination with medical articles or medical devices.
EP1286674B1 Composition for potentiating cancer chemotherapeutic agents The effect of cancer chemotherapeutic agents is potentiated by combination with mineral ascorbates, Vitamin C metabolites and/or a Vitamin C-derived furanone, illustratively a 4-hydroxy-5-methyl-3(2H)-furanone.
CA2445388C Stabilized medicine-releasing compositions A medicinal composition which has excellent storage stability and, even through long-term storage, is less apt to change in the rate of release of the pharmacologically active substance contained therein. The medicinal composition is one obtained by dissolving or dispersing a pharmacologically active substance and a pH-independent water-insoluble polymer in a molten low-melting substance. It is produced by dissolving or dispersing the pharmacologically active substance in a molten mixture of the low-melting substance and the pH-independent water-insoluble polymer and spraying and cooling the resultant liquid.
US7279458 Glycopeptide group is covalently linked to a pyridinium moiety of a cephalosporin group; reacting a glycopeptide containing (c6.c6.c6.c6.c6.c10n2.c13n2o.c13n2o ring) with a cephalosporin or salt in presence of a diacid This invention provides cross-linked glycopeptide—cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.
EP2651391A1 Pharmaceutical composition for oral administration intended to prevent misuse The field of the present invention is that of oral pharmaceutical forms, the composition of which makes it possible to prevent possible misuse of the active principle present therein. The present invention thus relates to a pharmaceutical composition for oral administration intended to prevent abuse of use at the expense of a third party.
US20080279963 Aqueous isotonic solution of hypohalous acid and halide salt; acidity pH; storage stability; active against three types of Staphlococcus Described herein is a physiologically-balanced, acidic solution. Typically the solution is prepared by a chemical reactions or by the electrolysis of a solution comprising a mixture of an inorganic salt to form a physiologically balanced solution. This invention also relates to methods for use of the solutions, including a specialized bandage which may be used in combination with the solutions, or optionally with other topically applied materials. A mixture of inorganic salts and, optionally minerals, is used in order to mimic the electrolyte concentration and mixture of body fluid in an isotonic state. The solution typically comprises of one halide salt of lithium, sodium, potassium, calcium, and other cations. Typically the halide is fluoride, chloride, bromide, or iodide, and most typically chloride. A typical electrolyzed solution of the present invention has a pH within the range of about 2 to about 5, an oxidation reduction potential within the range of about +600 mV to about +1200 mV, and hypohalous acid concentration in the range of about 10 ppm to about 200 ppm. The solution has bactericidal, fungicidal, and sporicidal properties. The composition of the invention is nontoxic and has antibacterial properties, and is useful in any application in which antimicrobial properties are desirable.
US20050075365 MAP (mitogen-activated protein) kinase inhibitors; osteoarthritis, rheumatoid arthritis, anticarcinogenic or antiischemic agents; reperfusion injuries, strokes or heart attack; autoimmune, skin, cardiovascular, brain, bone, neurodegenerative, respiratory system and nervous system disorders The present invention relates to novel triazolo-pyridines of the formula wherein X is >CH2, >NH, sulfur, >S═O, >SO2 or oxygen; wherein said >CH2 and >NH may optionally be substituted with a suitable substituent; R1 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; s is an integer from 0-4; R3 is R4, R5—(NR6)—, R5—S—, R5—(S═O)—, R5—(SO2)—, R5—SO2—NR6—, R5—(NR6)—SO2—, R5—O—, R5—(C═O)—, R5—(NR6)—(C═O)—, R5—(C═O)—NR6—, R5—O—(C═O)—, R5—(C═O)—O—, R5—CR7═CR8— or R5—C≡C_; such that the molecular weight of R3 is less than 500 AMU, preferably less than 250 AMU; R4, R5 and R6 are each selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; or a pharmaceutically acceptable salt thereof; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
WO2006070192A1 Thiazole and isothiazole derivatives that modulate the acivity of cdk, gsk and aurora kynases The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR5 or N; each of Q1 and Q2 is a carbon atom; Q3 is selected from S and CH; Q4 is selected from CR2 and S; provided that one of Q3 and Q4 is S and the other of Q3 and Q4 is not S; wherein when Q3 is S, there is a double bond between Q1 and Q4 and a double bond between Q2 and the adjacent ring nitrogen atom N; and when Q4 is S, there is a double bond between Q1 and Q2, and a double bond between Q3 and the adjacent ring nitrogen atom N; A is a bond or -(CH2)m-(B)n-; B is C=O, NRg(C=O) or O(C=O) wherein R1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R° is hydrogen or, together with NRg when present, forms a group -(CH2)p- wherein p is 2 to 4; R1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C1-8 hydrocarbyl group; R2 is hydrogen, halogen, methoxy, or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R3 and R4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, 0 and S; and R5 is hydrogen, a group R2 or a group R10 wherein R10 is as defined in the claims.The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.
US7410987 Treating pruritus or pain, particularly that caused by a rheumatic disease, by administering a 2-[o-(aminoalkoxy)phenyl])-3-acylbenzothiazoline, e.g., 3-Acetyl-6-chloro-2-[2-(3-(N-(2-hydroxyethyl)-N-isopropylamino)-propoxy)-5-methoxyphenyl]benzothiazoline A method of treating pain or pruritis comprising administering to a patient in need thereof a pharmaceutically effective amount of a κ opioid receptor agonist of the formula wherein R is an alkyl having an amino group as a substituent; and R1 is acyl.
WO2011137331A3 4-fluoro-4-arylpiperdin-1-yl derivatives as mu opioid function moderators 4-Fluoro-4-phenylpiperidin-1-yl μ antagonists of general structure (I) are useful as treatments of conditions or diseases associated with binding opioid receptors.
CN101269009A Novel anticancer injection A new anticarcinogenic sustained-release injection consists of sustained-release microballoon sphere and menstruum; wherein, the sustained-release microballoon sphere comprises anticarcinogenic active ingredient and sustained-release accessory material; the menstruum is special menstruum containing suspending agent. The anticarcinogenic active ingredient is the combination of cytotoxic drugs of fotemustine, bendamustine, tallimustine, carmustinum, nimustine, lomustine, semustine or ranimustine and adriamycin, epirubicin, melphalan, 4H peroxide cyclophosphamide, actinomycin D, vinorelbine or nolvadex, etc.; the sustained-release accessory material is selected from polylactic acid and the multipolymer or mixture thereof, mono-methyl polyethyleneglycol, polyethyleneglycol or polylactic acid multipolymer, EVAc, the multipolymer of fatty acid and decanedioic acid, etc.; the viscosity of the suspending agent is 100cp-3000cp (at the temperature of 25 DEG C-30 DEG C), the suspending agent is selected from sodium carboxymethyl cellulose, etc. The sustained-release microballoon sphere also can be made into sustained-release implant which can be injected and placed in tumor or around tumor and can release medicine at the local parts of the tumor for 30 to 40 days; therefore, the anticarcinogenic sustained-release injection can be separately united together with non-operativetreatment such as chemo-treatment and/or radiation treatment, etc. for application.
US7238720 Pharmaceutical use of N-carbamoylazole derivatives The present invention relates to use of 1-carbamoylazole derivatives as medicaments and pharmaceutical compositions containing 1-carbamoylazole derivatives as the active ingredient, based on their DPPIV inhibiting effects. The present invention provides a dipeptidyl peptidase IV inhibiting agent comprising a compound represented by the general formula (I):
WO2009010687A2 Target enzyme in the treatment of acne The invention relates to the use of an enzyme (DHRS9) as an acne research tool. The invention also relates to the use of said enzyme for the identification of a compound intended for the treatment of acne and/or any other disorder associated with hyperseborrhea, as well as to a method for identifying one such compound.
CN102000064A Medicinal application of flavanonol lignan in preparation glycosidase inhibitors The invention relates to medicinal application of flavanonol lignan in preparing glycosidase inhibitors, in particular to application of B-ring dioxane flavanonol lignan or pharmaceutically acceptable salts thereof in preparation medicines for inhibiting alpha-glucosidase and preventing type 2 diabetes. The flavone lignan has extremely obvious activity of inhibiting the alpha-glucosidase and has the activity strength of inhibiting the alpha-glucosidase at the concentration of 40 micrograms/milliliter of 93 percent; and a half inhibitory concentration test shows that: the strength of the flavone lignan of inhibiting the alpha-glucosidase is 1.2 times that of a positive contrast medicine acarbose. A pharmacodynamic result shows that the flavone lignan or the pharmaceutically acceptable salts thereof can be expected to serve as the glycosidase inhibitors, particularly serve as medicines for preventing the type 2 diabetes.
CN103443106A Novel octahydrothienoquinoline derivatives, pharmaceutical compositions comprising the derivatives and uses of the pharmaceutical compositions The present invention provides compounds represented by the general formula (I) having strong dopamine D2 receptor-stimulating activity, or pharmaceutically acceptable salts thereof, wherein where R1 is cyano, and the like; R2 and R3 are hydrogen, or the like; R4 is a C1-6 alkyl, or the like; R5 is a C1-6 alkyl, a halo-C1-6 alkyl, a cycloalkyl, a cycloalkyl C1-6 alkyl, an aralkyl, or the like; and R6 and R7 are respectively hydrogen or a C1-6 alkyl, a halo-C1-6 alkyl, a cycloalkyl, a C1-6 alkoxy C1-6 alkyl, a R12R13N-C1-6 alkyl, and the like, the invention also provides pharmaceutical compositions comprising the derivatives or the salts thereof; and provides uses pharmaceutical compositions.
CN1919259A External use medicine for treating stomatocace in children and preparation method thereof Disclosed is medicament for treating children's ulcerative stomatitis and process for preparation, wherein the medicament is prepared from the following raw materials (by weight portion): borax 18-20g, natural indigo 8-10g, and cow-bezoar 4-6g. The invention realizes easy material availability, simplified preparation, low cost, and quick effect.
WO2006057998A1 Binary antitumor compositions platinum (iv) derivatives The present invention provides combination compositions comprising Pt based compounds, including satraplatin, along with another chemotherapeutic agent such as temozolomide or lonafarnib. The combinations are useful for the prevention or treatment of cancer. Method of using the combinations to treat or prevent cancer are also provided.
US20120220659 Medicament having promoting action on hepatocyte proliferation A medicament for promoting proliferation of hepatocytes and liver regeneration, which comprises a polyprenyl compound such as 3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid as an active ingredient.
CN102988509A Preparation method and application of bone-knitting tablet The invention provides a preparation method of a bone-knitting tablet. The bone-knitting tablet is prepared by using 39g of szechuan lovage rhizome, 39g of radix aconiti preparata, 39g of Chinese angelica, 39g of frankincense stir-fried with vinegar, 39g of myrrh stir-fried with vinegar and 39g of forged natural coppers as bulk drugs and adopting supercritical extraction and microwave-assisted extraction modes. By adopting the method, the content of ferulic acid is greatly improved; and the invention also provides application of the bone-knitting tablet in preparation of drugs for inhibiting cell proliferation of mice leukemia cell NFS-60.
US20090047355 Process for producing pulverulent phytosterol formulations A process for the production of pulverulent phytosterol formulations, includes preparing an aqueous solution, suspension or dispersion of the phytosterol in an aqueous molecular dispersion or colloidal dispersion of a protective colloid and drying.
CN103145705A Beta-carboline alkaloid derivatives and their preparation method and medical use The invention provides beta-carboline alkaloid derivatives and pharmaceutically acceptable salts thereof, their preparation method, a pharmaceutical composition containing the beta-carboline alkaloid derivatives, and a medical use of the beta-carboline alkaloid derivatives and their pharmaceutically acceptable salts in drugs for treating neurodegenerative diseases such as Alzheimer's disease, Down's syndrome and Parkinson's disease.
WO2008117815A1 Inhibitor for cell death caused by endoplasmic reticulum stress or oxidation stress An inhibitor for cell death caused by endoplasmic reticulum stress or oxidation stress which contains, as the active ingredient, a carbazole derivative represented by the following general formula (I) or a pharmaceutically acceptable salt of the same: (I) wherein R1 represents a hydrogen atom or a C1-6 alkoxy group; and R2, R3 and R4 each represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group or a cyano group.
CN102600192A Compound terbinafine nanomedicine for treating skin diseases and preparation method thereof The invention discloses a compound terbinafine nanomedicine used for treating skin diseases. The grain size of the medicine is 1nm-10nm, and the compound terbinafine nanomedicine comprises the following components: 0.1%-10% of terbinafine, 0.1%-15% of eugenol, 0.1%-5% of erythromycin, 0.1%-10% of oil, 10%-40% of surfactant, 4%-20% of cosurfactant and the balance of distilled water, and the total percentage by weight of the components is 100%. The medicine disclosed by the invention has the advantages of small particle size, low viscosity, good liquidity, stable properties and better percutaneous permeability, and not only has a stronger curative effect on pet dermatomycosis, but also has a strong therapeutical effect on pet bacterial skin diseases and parasitic skin diseases. The compound terbinafine nanomedicine disclosed by the invention is easy to prepare, is low in energy consumption, and can be in mass production without special equipment. The compound terbinafine nanomedicine has wide application prospects in the aspect of pet skin disease treatment.
CN103172547A Preparation and application of sulfamide derivative The invention relates to preparation and application of a sulfamide derivative, and particularly provides a sulfamide derivative which has a structure of a general formula shown in the specification, wherein n is 0, 1, 2 or 3; R is C2-C4 straight-chain or branched-chain alkane, phenyl, cyclohexyl, o-methylphenyl, 3-pyridyl and 2-pyridylethyl. The compound can perfectly suppress the survival and growth of the cells SUM-159, HCC-1954 and MCF-7.
WO2006106307A1 Pyrimidine derivatives for use as anticancer agents A compound of formula (I), wherein the substituents are as defined in the text for use in inhibiting insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.
US7399780 pyridin-2-yl-1H-indole or pyrimidin-4-yl-1H-indole derivatives; enzyme inhibitor of glycogen synthase kinase-3; treating dementia, Alzheimer's Disease, Parkinson's Disease, amyotrophic lateral sclerosis, corticobasal degeneration, Down syndrome, Huntington's Disease The present invention provides new compounds of formula Ia and Ib: as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
WO2013179024A1 Sulfonyl piperidine derivatives and their use for treating prokineticin mediated diseases The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof : (I) in which m, n, W, X, Y, Z, R1, R2, R3 and R4 are as defined in the specification, for use in the treatment or prevention of a diseases o conition mediated by a prokineticin, such as psychiatric and neurological conitions.
US20090144841 Polymorphisms in the human gene for the multidrug resistance-associated protein 1 (MRP-1) and their use in diagnostic and therapeutic applications The present invention relates to a polymorphic MRP-1 polynucleotide. Moreover, the invention relates to genes or vectors comprising the polynucleotides of the invention and to a host cell genetically engineered with the polynucleotide or gene of the invention. Further, the invention relates to methods for producing molecular variant polypeptides or fragments thereof, methods for producing cells capable of expressing a molecular variant polypeptide and to a polypeptide or fragment thereof encoded by the polynucleotide or the gene of the invention or which is obtainable by the method or from the cells produced by the method of the invention. Furthermore, the invention relates to an antibody which binds specifically the polypeptide of the invention. Moreover, the invention relates to a transgenic non-human animal. The invention also relates to a solid support comprising one or a plurality of the above mentioned polynucleotides, genes, vectors, polypeptides, antibodies or host cells. Furthermore, methods of identifying a polymorphism, identifying and obtaining a pro-drug or drug or an inhibitor are also encompassed by the present invention. In addition, the invention relates to methods for producing of a pharmaceutical composition and to methods of diagnosing a disease. Further, the invention relates to a method of detection of the polynucleotide of the invention. Furthermore, comprised by the present invention are a diagnostic and a pharmaceutical composition. Even more, the invention relates to uses of the polynucleotides, genes, vectors, polypeptides or antibodies of the invention. Finally, the invention relates to a diagnostic kit.
CN101024654A Novel polymorphs and pseudopolymorphs of risedronate sodium Provided are novel polymorphs and pseudopolymorphs of risefronate sodium and risedronate disodium, methods for making them, and pharmaceutical compositions containing them.
WO2007147401A1 4-amino-3-arylamino-6-arylpyrazolo[3,4-d]pyrimidine derivatives, methods for their preparation and their use as antiviral agents The invention relates to 4-amino-3-arylamino-6-arylpyrazolo[3,4-d]-pyrimidine derivatives, method for their preparation and their use as antiviral agents. The object was to provide novel compounds which can be employed as agents for example for the treatment of picornavirus infections and which avoid problems of known medicaments, especially relating to resistance and intolerance. This object is achieved by compounds of the general formula I.
US20050004199 Treatment of inflammation with a combination of a cyclooxygenase-2 inhibitor and an integrin alpha-v antagonist The present invention provides for methods for treating or preventing an inflammatory disease or condition in a mammalian patient in need of such treatment comprising administering to said patient a cyclooxygenase-2 specific inhibitor in combination with an αVβ3, αVβ5? and/or αVβ6 integrin receptor antagonist in an amount effective to treat or prevent the inflammatory disease or condition. The present invention also provides for pharmaceutical compositions for the treatment or prevention of an inflammatory disease or condition. Further, the invention provides for the manufacture of a medicament useful in the treatment or prevention of an inflammatory disease or condition.
US20100076002 Method of Treating Atherosclerosis, Dyslipidemias and Related Conditions and Pharmaceutical Compositions A method of treating atherosclerosis is disclosed wherein nicotinic acid or another nicotinic acid receptor agonist is administered to the patient in combination with a DP receptor antagonist. The DP receptor antagonist is administered to reduce, prevent or eliminate flushing that may otherwise occur.
WO2012087389A1 Novel 19-nor-steroids and their use for treating progesterone-dependent conditions The subject matter of the instant invention is pertinent to the field of treatment of hormone-dependent conditions. New compounds and methods for treating these conditions are disclosed. Embodiments of the instant invention disclose methods for treating endometriosis, dysmenorrhea, breast cancer, uterine fibroids and endometrial hyperproliferation.
US20110172262 Compositions and methods for treating epilepsy Compositions and methods for treating epilepsy and epileptic syndromes are described herein. The compositions and methods include therapeutically effective amounts of one or more dimebolins, or pharmaceutically acceptable salts thereof.
US20060111443 Preventive therapeutic composition for muscular fatigue, pulled muscle and disease attributed thereto The present invention provides a composition for the inhibition of and promotion of recovery from muscular fatigue or muscular damage and diseases associated therewith, in particular, muscular fatigue or muscular damage caused by exercise stress and diseases associated therewith, and a composition for the prevention or treatment of myofibrosis during the restoration at the damaged part associated with or incidental to surgical injury or surgical procedure, which are characterized by comprising as an active ingredient N-(3,4-dimethoxy-cinnnamoyl)anthranilic acid (generic name: tranilast) or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, and a method for use thereof.
CN101884619A Zolpidem tartrate controlled-release pellet and preparation method thereof The invention provides an officinal composite containing zolpidem tartrate, and the weight of the active ingredients of the officinal composite is between 1mg and 20mg. The invention is characterized in that the officinal composite is a controlled-release pellet which mainly consists of a pill core and a controlled-release layer with a controlled-release function or consists of a faster-working quick-release outer layer part, a controlled-release layer maintaining slow release and a pill core. The preparation prepared by the invention can prolong drug release time by 6h and play roles in reducing blood concentration fluctuation and prolonging drug action time.
US20100305055 Combinations of polyene fungicide with cationic surfactants A solid composition comprising a cationic surfactant, such as the ethyl ester of the lauramide of the arginine mono-hydrochloride (LAE) and a polyene fungicide such as natamycin is provided. The solid composition is the basis for providing solutions of natamycin of increased concentration. The solid composition may be used for providing a dispersion of natamycin in a suitable liquid, such as tap water or an organic solvent. The dispersion may be further diluted with water. This leads to a solution of natamycin in water. The combination of the cationic surfactant and the polyene fungicide displays a biological effect which is stronger than the effect of each of the two components alone.
US8815287 Opiod agonist formulations with releasable and sequestered antagonist Disclosed are oral dosage forms, comprising (i) a therapeutically effective amount of an opioid agonist; (ii) an opioid antagonist in releasable form; and (iii) a sequestered opioid antagonist which is not released when the dosage form is administered intact, and methods thereof.
WO2011085201A1 Fumagillol type compounds and methods of making and using same The disclosure provides a fumagillol type compound and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.
CN101234106B Use of imidazolone compounds for treating cardiovascular and cerebrovascular diseases The invention relates to a medicine field, in particular relates to application of (Z)-1-methyl-1, 5-dihydro-2-amido-5-(4-(mesyl) benzal)-4H-imidazole-4-ketone and pharmaceutically acceptable salt thereof in the treatment of cardiovascular and cerebrovascular diseases of mammals; the compound and the salt of the compound can effectively prohibit formation of thrombus and are used for preventing or curing diseases such as coronary heart disease, atherosclerosis, artery and vein thrombosis, angina, myocardial infarction, coronary heart disease, myocarditis, ischemic cardiomyopathy, myocardial infarction, cardiovascular complications of diabetes, cerebral haemorrhage, cerebral thrombosis, cerebral embolism, cerebral infarction, brain stroke, lacunar infarction, transient ischemic attack, cerebral arteriosclerosis and peripheral vascular diseases such as obstructive vasculitis, aortoarteritis, hypercholesterolemia, or high blood lipids, etc.
CA2379560C Purine derivatives inhibitors of tyrosine protein kinase syk Compounds of formula (I) in free or salt form, where X, R1, R2, R3 and R4 are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of inflammatory or obstructive airways disease.
WO2011104338A1 Halogen or cyano substituted thieno [2,3-d]pyrimidines having mnk1/mnk2 inhibiting activity for pharmaceutical compositions The present invention relates to novel thienopyhmidine compounds of general formula (I), pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
CN101732368A Medicinal liquid for treating burn and scald The invention relates to a medicinal liquid for treating a burn and a scald, which is characterized in that: the medicinal liquid is prepared from the following raw materials in percentage by weight: 20 to 40 percent of halomine and 60 to 80 percent of sesame oil. When the medicinal liquid is used, a wound is cleaned and disinfected firstly, then the medicinal liquid is applied, and the wound is preferably wrapped by sterile gauze after the medicinal liquid is applied. The medicinal liquid is convenient and easy to use and has obvious effects of treating the burn and the scald.
WO2009071895A1 Fused thiazole and thiophene derivatives as kinase inhibitors A series of fused bicyclic thiazole and thiophene derivatives which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, and in the 4-position by hydroxy, oxo or an amine moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. (I)
US20100035864 2,2-Dimethyl-4-oxo-4-(4-{4-[(2-phenyl-5-trifluoromethyl-oxazole-4-carbonyl)-amino]-phenyl}-[1,4]diazepan-1-yl)-butyric acid, hydrochloride; obesity, type II diabetes mellitus and metabolic syndrome Provided herein are compounds of the formula (1): as well as pharmaceutically acceptable salts thereof wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type 11 diabetes mellitus and metabolic syndrome.
WO2007084059A1 A food composition comprising amino acids The invention relates to a food composition comprising an amino acid part having at least the amino acids leucine, isoleucine, valine, threonine and lysine in an amount of from about 35 to about 90 g/100 g of the total amount of the amino acid part as well as a method how to produce said food composition. The invention also relates to different food products comprising said food composition.
WO2006103551A1 Controlled release formulations of oxycodone The present invention relates to controlled release formulations of oxycodone with one or more hydrophilic controlled release polymers, and processes for their preparation.
WO2014096423A1 Therapeutically active pyrazolo-pyrimidine derivatives A series of pyrazolo[3,4-d]pyrimidine derivatives that are substituted at the 4- position by a diaza monocyclic, bridged bicyclic or spirocyclic moiety, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseasesand malaria; and organ and cell transplant rejection.
WO2014008992A1 Pyrimidine pyrazolyl derivatives The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases (I).
CN102247320A Etoposide long-circulating emulsion and preparation method thereof The invention belongs to the field of medicinal preparations, and relates to an etoposide long-circulating emulsion for injection, and a preparation method thereof. The etoposide long-circulating emulsion comprises etoposide, fluid oil, emulsifiers, polyethylene glycol (PEG) modified esters and the like, and has the characteristics of high entrapment rate, good stability and low toxicity. The etoposide long-circulating emulsion improves the solubility and the stability of etoposide, reduces irritation effects of etoposide on blood vessels, prolongs cycle time of etoposide in blood, and improves distribution of etoposide in vivo thus improves drug curative effects. The preparation method of the etoposide long-circulating emulsion solves the carrying problems of drugs with poor water-solubility and fat-solubility and realizes stable preservation and no drug precipitation. The preparation method has the characteristics of simple process, low cost and good applicability for industrializedproduction.
US20120315289 Non-polysaccharide constituent of genus Dendrobium, usage for the non-polysaccharide constituent of genus Dendrobium and extracting method thereof The present invention discloses a non-polysaccharide constituent for positively regulating the immune system in the therapy of allergic diseases. The non-polysaccharide constituent is extracted from genus Dendrobium by incubating in alcohol and extracting using solvents with different polarity.
WO2006040178A1 Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to madulation of the dopamine d3 receptor The present invention relates to aromatic compounds of the formula (I), wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, -CH=N-, -CH=CH- or -N=CH-; A is CH2i O or S; E is CR6R7 or NR 3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C,-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4 -cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
US20120157476 Oxime compounds The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
CA2068224C Novel potent inducers of terminal differentiation and method of use thereof The invention provides compounds, several of which belong to a class having two or more nonpolar components connected by a polar group and having polar groups on the termini of the compound. The invention also concents a method of selectively inducing termini differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effective to selectively induce terminal differentiation. Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound in an amount effective less than an amount which would cause toxicity in the patient.
EP2480287A2 Dry powder combination of tiotropium The present invention relates to a pharmaceutical composition containing tiotropium formulated with an effective amount of a cromolyn derivative used for the treatment of respiratory disease by inhalation route.
US20110070272 Materials and Methods for Modulating Metabolism The subject invention provides materials and methods for modulating a variety of biological factors to treat biological conditions associated with the factors. In one embodiment of the invention, a cysteamine compound is administered to a patient to treat hypercholesterolemia and/or complications associated with hypercholesterolemia. In another embodiment, a cysteamine compound is administered to a patient to prevent the onset of diabetes in an at-risk patient and/or treat or prevent the onset of diabetes-associated complications.
CN103191319A Medicine for treating epistaxis and preparation method thereof The invention discloses a medicine for treating epistaxis and a preparation method thereof. The medicine is prepared from cape jasmine, radix ophiopogonis, lalang grass rhizome, herba portulacae, roots of madder, liquorice, donkey-hide gelatin and the like according to a certain weight ratio. The medicine disclosed by the invention has the functions of warming channel and promoting lactation, clearing away heat and reducing fire, and cooling blood and stopping blooding, is good in curative effect and high in recovery rate in treatment of epistaxis, and fast becomes effective.
CN101073625A Medicinal composition with anti-infective and anti-inflammatory functions The invention is concerned with the compound medicine for dishimishing infenction and inflammation. It includes: Shegan total flavonoids and andrographolidume or derivatives thereof with the weight ratio of 1:20 to 20:1(endpoint included), which can execute all kinds of preparation with other supplementary materials or excipients that are pharmacy acceptable.
US20100317719 Antisense Oligonucleotides (ODN) Against SMAD7 and Uses Thereof in Medical Field The invention relates to antisense oligonucleotidic sequences (ODN) against Smad7 suitably modified, and their uses in medical field as therapeutic biological agents, in particular in the treatment of chronic inflammatory bowel disease, such as Crohn's disease and ulcerative colitis.
CN103099805A Application of isosteviol derivative H14 in preparation of antitumor medicaments The invention belongs to the fields of chemical industry and medicine, and relates to application of an isosteviol derivative H14 in preparation of antitumor medicaments. In the application of the H14 in preparation of antitumor medicaments, tumor cells include liver cancer cells, leukemia cells, lung adenocarcinoma cells and pancreatic cancer cells. The H14 belongs to a natural product, is low in toxic and side effect, high in bioavailability and stable in property, and has clinical use value. The small-molecule compound provided by the invention can be developed as a new antitumor medicament or an auxiliary component thereof, has remarkable tumor inhibition effect, and is green and environment-friendly, thereby providing a new way and means for treating and curing tumors.
US20110136760 Kinase Inhibitors Useful for the Treatment of Myleoproliferative Diseases and other Proliferative Diseases The present invention is concerned with novel compounds useful in the treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds. The preferred compounds are active small molecules set forth in formulae Ia-Iww.
US6919449 Process for the preparation of cephalosporin intermediate and its use for the manufacture of cephalosporin compounds The present invention relates to a method for the preparation of cephalosporin antibiotic of the formula (II), which comprises hydrolyzing and halogenating the ester of formula (III) by photochemical irradiation in one pot using a halogenating agent in the absence or presence of a solvent, to produce compound of formula (I), activating the 4-halogeno-2-substitutedimino-3-oxo-butyric acid of formula (I) using conventional activation agents gives compound of formula (IV), condensing the activated compound of the formula (IV) with 7-amino cephem derivative of the formula (V) to produce a compound of formula (VI), and cyclizing the compound of formula (VI) with thiourea to give cephalosporin compounds of the formula (II).
CN102795953A Method for synthesizing caffeic acid amide derivative by using caffeic acid and sulfanilamide drug as raw materials and application The invention discloses a method for synthesizing caffeic acid amide derivatives by using caffeic acid and sulfanilamide drugs as raw materials and an application. The synthetic method comprises the following steps: dissolving caffeic acid in acetic anhydride, reacting with pyridine, tetrahydrofuran and sulfanilamide drugs in order to obtain amide compound crude products, performing procedures of filtration, washing, recrystallization and the like to obtain the caffeic acid amide derivatives. The extraction method of the invention is simple, easy to operate, and high in purification rate. The caffeic acid amide derivatives synthesized through tests have inhibition effect on pneumococcus, escherichia coli, pseudomonas aeruginosa, shigella dysenteriae, and salmonella, and are applicable to the preparation of drugs with bacteriostatic effect.
US20100317679 Substituted aryl-fused spirocyclic amines Substituted Aryl-fused Spirocyclic Amines of the formula (I): are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
US20110105595 Novel promoter and viral vector containing the same The invention constructs an activating KRASmutant but not p53-responsive promoter and generates an E1B-55kD-deleted (ΔE1B-55kD) adenovirus, harboring a transcriptionally activating transgene and holding lytic replication ability in the tumor cells with activating KRASmutant. The adenovirus of the invention can be used in the treatment of cancers.
CN102731596A Flavonoid glycoside compound, its preparation method and application Belonging to the field of natural pharmaceutical chemistry, the invention provides a flavonoid glycoside compound, its preparation methods and application of the compound in preparation of anti-inflammatory and antioxidant substances. The structural formula of the compound is shown as the following.
EP1734957A2 Thiazole sulfonamide compounds for the treatment of neurodegenerative disorders The present invention relates to compounds of the Formula (I) wherein R1, R2, R3, R4, m, n and p are as defined. Compounds of the Formula (I) have activity inhibiting production of Aβ-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula (I).
EP1658064A2 Combinations of vasoactive agents, their use in the pharmaceutical and cosmetic field, and formulations containing them This invention relates to combinations of vasoactive substances which act at venous or arterial level with phosphodiesterase inhibitors including phosphodiesterase V, in particular: visnadin or esculoside; at least one compound selected from icarin or derivatives thereof or extracts containing it, Gingko biloba dimeric flavones either in the free form or complexed with phospholipids, amentoflavone; at least one compound selected from escin, escin beta-sitosterol complexed with phospholipids, sericoside, sericoside complexed with phospholipids or Centella asiatica extract in the free form or complexed with phospholipids. The formulations according to the invention are useful in reducing parmiculopathy and problems associated with venous insufficiency of the lower limbs.
WO2009130422A2 N-acylthiourea and n-acylurea inhibitors of the hedgehog protein signalling pathway The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.
US20110086109 Low ether compositions and delivery apparatus A low ether gel composition for application to skin comprising a keratolytic agent, in particular salicylic acid, and comprising a nitrocellulose and one or more volatile ingredients, which forms a film on contact with skin adequate to form a protective barrier for the keratolytic agent for a period of time necessary to provide treatment to the skin; methods of treating using such compositions, and dispensers containing such compositions.
CN102688189A Lurasidone medicine composition and preparation method thereof The invention discloses a lurasidone medicine composition and a preparation method thereof. Concretely, the lurasidone medicine composition disclosed by the invention comprises the lurasidone shown in the formula (I), polyhydroxy alcohol and water. The invention also relates to the application of the lurasidone medicine composition in preparing a medicine for psychosis, and a method for preparing the lurasidone medicine composition. The method comprises the following steps of: dissolving the lurasidone in a proper amount of polyhydroxy alcohol; adding water and optional other additives; and adding polyhydroxy alcohol until the total amount of the prescription is obtained; optionally sterilizing or removing bacteria of the liquid composition; and sealing and packing. The lurasidone medicine composition disclosed by the invention is suitable for old patients and patients uncooperative in taking medicines.
CN101732308A New application of leptomycin B, pharmaceutical compositions and products thereof The invention relates to new application of leptomycin B, pharmaceutical compositions and products thereof. The invention specifically relates to the application of leptomycin B or pharmaceutically acceptable salt or ester thereof in preparing medicaments for reversing multi-drug resistance of cancer. By using the scheme of the invention, the multi-drug resistance of the multi-drug resistance of cancer cell can be effectively reversed for anti-tumor therapy.
US20090286871 Use of a plant oil product as an agent for increasing the synthesis of skin lipids The present invention relates to the use of a plant oil product as an agent for increasing the synthesis of skin lipids, especially the lipids of the epidermal skin barrier, in or for the preparation of a cosmetic, pharmaceutical or dermatological composition. The invention also relates to a method for cosmetic treatment with a cosmetic, pharmaceutical or dermatological composition for increasing the synthesis of skin lipids, especially the lipids of the epidermal skin barrier, and to the use of the plant product as a food additive.
CN1977835A Monomer medicine for treating ankylosing spondylitis The present invention relates to an application of theanine in preparation of medicine or health-care product for curing spondylitis ankylopoietica, belonging to the field of medicine or health-care product technology. It uses existent industrial theanine product as raw material and utilizes conventional medicine or health-care production equipment to prepare the invented product.
EP2571515A2 Methods and assays for treating subjects with shank3 deletion, mutation or reduced expression Methods and assays are disclosed for treating subjects with 22ql3 deletion syndrome or SHANK3 deletion, mutation or reduced expression, where the methods comprise administering to the subject insulin-like growth factor 1 (IGF-1), IGF-1-derived peptide or analog, growth hormone, an AMPAkine, a compound that directly or indirectly enhances glutamate neurotransmission, including by inhibiting inhibitory (most typically GABA) transmission, or an agent that activates the growth hormone receptor or the insulinlike growth factor 1 (IGF-1) receptor, or a downstream signaling pathway thereof.
CN101757008A Purpose of ginsenoside Rg1 The invention discloses applications of 1.25-40mg, 2.5-40mg, 10-30mg and 20mg/kg of ginsenoside Rg1 in preparation of antithrombotic medicine. The dose-effect relationship shows that the ginsenoside Rg1 has good pharmacological effect, which further proves that the invention has wider safety range.
US20130079377 Aryl or N-heteroaryl Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands The invention relates to aryl or N-heteroaryl substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
CN101933917A Application of Hyperforin derivant in preparing drugs The invention discloses an application of Hyperforin ethyl ester with a structure I1 and/ or Hyperforin-N, N dicyclohexyl ammonium with a structure I2 in preparing drugs capable of treating tumor. The pharmacological pharmacodynamics experiment proves that the Hyperforin ethyl ester and the Hyperforin-N, N dicyclohexyl ammonium of the invention have the action of specific proliferation inhibition, apoptosis induction, cell cycle influence and the like on human tumor cells cultured in vitro and provide new drug selection for clinic tumor therapy.
WO2005094831A1 Sustained-release tablet formulation The invention provides a sustained-release tablet that can release caffeine and other xanthine derived stimulants at a nearly constant rate. The tablet comprises a hydrophilic polymer of high molecular weight and in one embodiment, the tablet includes caffeine and poly(ethylene oxide) of molecular weight of about 4 x 106 to 8 x 106. Sustained delivery of caffeine and other xanthine-derived stimulants is possible with a low concentration of the polymer and moreover, a wide range of concentration of caffeine and other stimulants can be released at a nearly constant rate.
CN101919871A Application of cyclophosphamide and panaxoside in preparing medicine for treating condyloma acuminatum The invention discloses an application of cyclophosphamide and panaxoside in preparing a medicine for treating condyloma acuminatum. In the application of the cyclophosphamide combined with the panaxoside in preparing the medicine for treating the condyloma acuminatum, the medicine containing low doses of the cyclophosphamide and the panaxoside is taken by patients with condyloma acuminatum, can effectively mobilize the body to generate immune response which can effectively resist human papillomavirus (HPV), removes the human papillomavirus infected by the patients with the condyloma acuminatum, generates favorable therapeutic action on the condyloma acuminatum, can prevent the condyloma acuminatum from recurring, does not generate effects on the liver and kidney functions of the patients with the condyloma acuminatum, has no obvious toxic and side effects, and displays the unique advantages of the cyclophosphamide combined with the panaxoside in treating the condyloma acuminatum.
EP1230920B1 Use of food materials in preventing and ameliorating metabolic bone diseases Drinks and foods having a bone formation function which contain as the active ingredient an efficacious amount of a culture of a propionic acid bacterium and/or a lactic acid bacterium containing 2-amino-3-carboxy-1,4-naphthoquinone; and preventives/remedies for metabolic bone diseases which contain as the active ingredient a naphthoquinone compound selected from the group consisting of 2-amino-3-carboxy-1,4-naphthoquinone, 1,4-naphthoquinone, 2-hydroxy-1,4-naphthoquinone, 2,3-dichloro-1,4-naphthoquinone, 5-hydroxy-1,4-naphthoquinone, 2-(α-hydroxy-δ-methylpentenyl)-5,8-dihydroxy-1,4-naphthoquinone and salts thereof. The above-described culture and naphthoquinone derivatives promote the bone metabolism, thereby elevating bone mass and bone strength.
US20060025360 Human cervical cancer protooncogene and protein encoded therein A human cervical cancer 1 protooncogene having a base sequence of SEQ ID:1 or a fragment thereof is overexpressed in various cancer tissues and can be used in diagnosing various cancers and an anti-sense gene complementary thereto can be used in treating cancers.
CN103127051A Application of curcumenol in anti-tumor drug preparation The invention belongs to the field of chemical engineering and medicine, and relates to an application of curcumenol in anti-tumor drug preparation. The present invention provides an application of curcumenol in anti-tumor drug preparation, wherein tumor cells comprise liver cancer cells, leukemia cells and pancreatic cancer cells. The curcumenol belongs to natural products, and has characteristics of high bioavailability, stable property, and clinical use value. With application of the small molecule compound as a new anti-tumor drug or an auxiliary component thereof to be developed, advantages of significant tumor inhibition effect and green environmental protection are provided, and a new way is provided for treatment and cure of tumors.
WO2009069838A1 A composition for promoting osteoblast differentiation comprising berberine. Berberine (BBR) stimulates Runx2 activity via p38 MAPK in osteoblasts and enhances COX2 expression through the p38 MAPK-RUNX2 pathway, resulting in an increase in osteoblast differentiation, which was confirmed in an ex vivo new bone formation study. Therefore, BBR may be a potential therapeutic agent to treat bone-related disorders including osteoporosis.
EP1949890A2 Implantable gel compositions and method of manufacture Methods and compositions for reducing the burst of beneficial agent from implantable systems is described. Such systems utilize compressed particulates of a beneficial agent, optionally mixed with a dissolution rate modulator or an agent exhibiting a characteristic of low solubility in water, such as a mixture of stearic acid and palmitic acid, dispersed throughout a bioerodible and biocompatible carrier.
US20100234376 [4,5']Bipyrimidinyl-6,4'-Diamine Deriviatives as Protein Kinase Inhibitors The invention provides a novel class of compounds of the Formula I: in which the symbols have the meanings given in the description and claims, to pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of FGFR3 kinase.
CN1771919A Compound soft lutein capsule and its prepn process The present invention discloses one kind of composite soft lutein capsule and its preparation process. The content in each capsule includes lutein1-10 mg, alpha-linolenic acid 100-300 mg, vitamin A 0-5 mg and vitamin E 0-7.5 mg; and the capsule covering consists of gelatin, glycerin, water, and opacifier or edible color. The lutein is prepared through supercritical CO2 extraction process, and has no pollutant and organic solvent residue. The composite soft lutein capsule product has stable quality and high bioavailability, and has certain preventing and treating effect on senile macular degeneration, cataract and cardiac and cerebral vascular diseases.
EP2357173A1 New alkyne compounds with MCH-antagonistic activity and medicaments containing them Amino substituted alkyne derivatives (I), are new. Amino substituted alkyne derivatives of formula R 1>(R 2>)-N-X-Y-Z-Ctriple boundC-W-A-B' (I), their tautomers, diastereomers, enantiomers, mixtures and salts are new. R 1>, R 2>e.g. H or 1-8C alkyl or 3-7C cycloalkyl (both optionally substituted), where one CH 2 at position 3 or 4 of a 5-7 membered cycloalkyl is optionally replaced, or phenyl or pyridyl (both optionally substituted), or R 1> + R 2>e.g. 2-8C alkylene in which 1 or 2 CH 2 are optionally replaced by CH=N or CH=CH or, provided heteroatoms are not adjacent, by e.g. oxygen, sulfur, SO, SO 2, and optionally substituted; X : e.g. 1-8C alkylene in which one CH 2 is replaced by CH=CH or ethynylene or 1 or 2 CH 2 are replaced, or X + NR 1>R 2>heterocyclyl; W, Z : e.g. a single bond, 1-4C alkylene optionally having CH 2 not adjacent to the alkynyl group replaced by e.g. oxygen; Y : Cy; Y + X + N + R 1>heterocyclyl, or X + Y : carbocyclyl or heterocyclyl; A : Cy; B' : e.g. Cy, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 1-3C alkyl substituted by 3-7C cycloalkyl or cycloalkenyl, 2-3C alkenyl or 2-3C alkynyl substituted by 3-7C cycloalkyl, where one or more C are optionally substituted, and Cy : e.g. saturated 3-7 membered carbocyclyl, unsaturated 4-7C carbocyclyl, phenyl, saturated 4-7 or unsaturated 5-7 membered heterocyclyl containing one N, O or S heteroatom, saturated or unsaturated 5-7 membered heterocyclyl containing at least 2 N or one or two N and one O or S heteroatoms, aromatic 5-6 membered heterocyclyl containing one or more N, O and/or S heteroatoms, where the 4-7 membered rings are optionally fused to phenyl or pyridyl through two adjacent C, the 5-7 membered rings contain 1 or 2 non-adjacent CH 2 replaced by CO, C(=CH 2), SO or SO 2, the saturated 6-7 membered rings optionally form a bridged system containing (1-4C alkyl)imino or methylene (optionally substituted by 1 or 2 1-4C alkyl) and the cyclic groups are optionally substituted. Full definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are also included for the preparation of (I). - ACTIVITY : Anorectic; Eating-Disorders-Gen.; Anabolic; Immunomodulator; Antidiabetic; Ophthalmological; Neuroprotective; Nephrotropic; Cardiant; Antiarteriosclerotic; Hypotensive; Antiarthritic; Antilipemic; Antidepressant; Anticonvulsant; Nootropic; Uropathic; Tranquilizer; Hypnotic; Sedative; Endocrine-Gen.; Uropathic. - MECHANISM OF ACTION : Melanin concentrating hormone-1 receptor antagonist. In a MCH-1 receptor binding assay, results showed that 5-(4-bromophenyl)-2-[4-(2-pyrrolidin-1-ylethoxy)phenylethynyl]-pyrid ine (Ia) exhibited an IC 50 value of 8 nM.
CN1775813A Carboxy methyl schizophllan polysacharide preparing method and its use for use in cosmetics and anticancer drugs The invention discloses a carboxymethyl crack pleat polysaccharide preparation method and its application in cosmetic and antineoplastic. Neutral crack pleat polysaccharide is transformed into carboxylic acid sodium salt with negative electric charge by its carboxy methylation in the invention. And this not only can improve its solubility, but also can keep its good rheological behavior and antineoplastic activity. The invention uses the chemical agent to substitute the carboxyl of the polysaccharide, and controls molecular weight and degree of substitution of the carboxymethyl crack pleat polysaccharide by reaction condition to make it have good solubility and antineoplastic activity. And it can apply in cosmetic, antineoplastic, food, and so on.
US6849658 Biaromatic compounds and pharmaceutical and cosmetic compositions comprising them The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar; R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S; R4 is aryl radical; R5 is H, halogen, C1-C20 alkyl or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r′)(r″) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r′ and r″ are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of the compounds of formula (I).
US20100143507 Carboxylic acid inhibitors of histone deacetylase, gaba transaminase and sodium channel The present invention relates to new carboxylic acid inhibitors of histone deacetylase, GABA transaminase, and/or sodium channel activity, pharmaceutical compositions thereof, and methods of use thereof.
US20100152249 Compositons and method for treatment of mood and cognitive impairments Compositions, manufacture, and methods for diagnosis and treatment of subjects exhibiting mood disorders and/or being at risk of cognitive impairment.
CA2563325C Oral modified-release lozenges and their preparation method This invention relates to oral modified-release lozenges characterized in that they contain micronized active components as antidiabetic and modified-release agents. This invention also provides such lozenges preparation method. Compared with conventional formulations comprising the same active components, the oral modified-release lozenges of this invention possess more excellent solubility, more persistent absorptivity, and more effective curative effect.
CN103386130A ACE inhibitor/thiazide diuretic/5-methyltetrahydrofolate pharmaceutical composition and applications The invention relates to a pharmaceutical composition containing combination of an angiontensin converting enzyme (ACE) inhibitor, a thiazide diuretic and 5-methyltetrahydrofolate, and applications thereof. The pharmaceutical composition comprises: the angiontensin converting enzyme inhibitor in medicinal dosage, the thiazide diuretic in medicinal dosage, 5-methyltetrahydrofolate in medicinal dosage, and a pharmaceutical acceptable carrier. The invention provides an application of the pharmaceutical composition to preparing medicaments for treating hypertension and preventing, treating or delaying target-organ damage caused by hypertension; also the invention provides an application of the pharmaceutical composition to preparing medicaments for reducing cerebrovascular accident danger caused by hypertension. Through enforcement of the pharmaceutical composition, the pharmaceutical composition with specific applications is provided for patients, and helps to increase medication compliance of the patients, improve cure effect and reduce medical cost.
US8067000 Cancer treatment with endothelin receptor antagonists The present invention relates to therapeutic protocols and pharmaceutical compositions designed to treat and prevent cancer. More specifically, the present invention relates to a novel method of treating cancer using antagonists to the endothelin B receptor (ETB) or inactive mimic forms of endothelin-1. The pharmaceutical compositions of the invention are capable of selectively inhibiting the early events associated with the development of cancer. The present invention further relates to screening assays to identify compounds which inhibit ETB activation.
US20080274207 packaging solution that maintains a consistent level of antimicrobial metal salt; little of the antimicrobial metal salt is lost during autoclaving and storing the contact lens This invention relates to solutions for packaging ophthalmic devices comprising at least one antimicrobial metal salt which prevent the loss of said antimicrobial metal salt during autoclaving and storage.
WO2006121359A1 Epirubicine hydrochloride for treating hepatitis c virus Second medical application of epirubicine hydrochloride according to the invention is characterized by its use as an active substance inhibiting the hepatitis C virus (HCV) replication while having low toxicity in Huh7 cells. Epirubicine hydrochloride is employed in therapy of HCV infections. Pharmaceutically accepted forms of the anti-HCV drug, best if applied as water solutions suited for injections, according to the invention, are distinguished by containing epirubicine hydrochloride applied at cumulated, antiviral therapeutic doses comprising 1 - 100 mg/m2 of body surface (0,02 - 2 mg; 0,0344 - 3,44µM per kg of body weight).
CN101670061B Veterinary drug for treating respiratory tract infection of poultry and preparation method thereof The invention discloses a veterinary drug for treating respiratory tract infection of poultry and a preparation method thereof. The veterinary drug is prepared mainly from the following materials by weight part: 30-120 parts of radix stemonae, 10-120 parts of scutellaria baicalensis, 30-210 parts of giant knot weed, 10-60 parts of indigo naturalis, 10-60 parts of artificial bezoar, 10-40 parts ofborneol, 10-90 parts of realgar, 10-60 parts of liquorice, 30-120 parts of platycodon root, 90-210 parts of cyrtomium fortunei, 30-120 parts of blackberry lily, 10-210 parts of dried toad, 150-420 parts of radix isatidis and 1-10 parts of bromhexine hydrochloride. The veterinary drug is prepared by grinding, screening and evenly mixing the materials, and grinding the materials by a superfine pulverizing technology into submicron powder and packing. The veterinary drug is mainly used for treating respiratory diseases of poultry caused by the bacterial viruses such as infectious bronchitis of chicken, infectious laryngotracheitis, newcastle disease and influenza. The invention has the advantages of rapid drug effect, favorable effect and little remaining charge, has simple preparation method and is easy for promotion and application.
EP2486921A1 Reducing Side Effects of Tramadol A pharmaceutical composition comprising a pharmaceutically-acceptable carrier, a tramadol material and a phosphodiesterase (PDE) inhibitor, a pharmaceutical composition comprising a pharmaceutically-acceptable carrier, a phosphodiesterase (PDE) inhibitor and an opioid antagonist, a kit comprising a container holding a tramadol material and a phosphodiesterase (PDE) inhibitor; or a first container holding a tramadol material and a second container holding a phosphodiesterase (PDE) inhibitor and a kit comprising one or more containers, each of which holds a tramadol material, a phosphodiesterase (PDE) inhibitor, an opioid antagonist or a combination of two or more of the foregoing.
CN102552402A External medicine for treating rheumatic diseases The invention discloses an external medicine for treating rheumatic diseases, which is prepared from Chinese ephedra, cassia twig, asarum, angelica root, leech, centipede, scorpion, frankincense, myrrh, camphor, borneol and Cynanchum paniculatum. The external medicine has an obvious treating effect on various rheumatic diseases and has the advantages of convenience and rapidity, short curing period and no toxic and side effect, and the effective rate reaches 100%.
US20110046139 Benzocycloheptane and benzoxepine derivatives The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof
EP2412707A2 3-[2-(3-Amino-2-oxo-2H-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives and their use as caspase inhibitors The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.
EP2277884A1 Anthracycline antibiotic derivatives with high activity, preparation methods and uses thereof The present invention relates to tetracyclic anthraquinone antibiotic derivatives with anticancer activity. The tetracyclic anthraquinone antibiotic derivatives as provided in the present invention have the same or higher activity than that of the known drugs such as doxorubicin, daunorubicin and the like in the cellular level while having better tolerance than that of doxorubicin and daunorubicin in the animal body.
US20130079373 Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands The invention relates to substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
US20050054723 Administration to the individual of a prostaglandin analogue selective for the EP2 prostanoid receptor in combination with an alpha-adrenergic agonist Prostaglandin-induced increased pigmentation of the iris can be avoided, or significantly reduced, when using a selective EP2 prostanoid receptor agonist in combination with an alpha-adrenergic agonist. Methods and compositions for the treatment of glaucoma and ocular hypertension are described.
US20100069478 Isoflavone derivatives and uses thereof Isoflavone derivatives are provided comprising a carboxyalkylene moiety linked via its alkylene chain to the aromatic ring and via its carboxy group to an aminoalkyleneamino residue, which, in turn, is covalently linked to a functional group B. The isoflavone derivatives are preferably derived from biochanin A, genistein, and daidzein, and the functional group B is preferably an amino protecting group. These isoflavone derivatives are useful for treating or preventing diseases or disorders associated with estrogen receptor functioning.
CA2229202C Methods for identifying antagonist or agonist to human opioid receptor-like 1 "orl1" The present invention is related to nucleic acid molecules, the peptides encoded by said nucleic acid molecules and the inhibitors directed against said nucleic acid molecules or said peptides. The present invention concerns also the pharmaceutical composition, the diagnostic and/or dosage device comprising said products and methods for identifying the inhibitors according to the invention.
US20110262437 Use of erbb4 as a prognostic and therapeutic marker for melanoma It is disclosed herein that members of the protein tyrosine kinase (PTK) family are highly mutated in patients with melanoma. Described herein are novel somatic mutations in the ERBB4 gene that result in increased kinase activity, transformation ability and anchorage-independent growth. These ERBB4 mutations contribute to the tumorogenicity of melanoma. Thus, provided herein is a method of predicting the prognosis of a patient with melanoma by detecting the presence or absence of a mutation in the ERBB4 gene. In some examples, the ERBB4 mutation is selected from G949A, G1354A, G1624A, C1630T, G1687A, G2506A and G2614A (numbering based on SEQ ID NO: 1). Also provided are methods of selecting a patient as a candidate for treatment with an ERBB4 and/or PI3K/AKT pathway inhibitor, and a method of identifying a therapeutic agent for the treatment of a subject diagnosed with melanoma. Oligonucleotides that specifically hybridize with an ERBB4 nucleic acid molecule comprising a novel mutation, and arrays comprising such oligonucleotides, are also provided.
CA2316888C Methods of inactivating bacteria including bacterial spores Methods for inactivating bacteria including bacterial spores using an oil-in-water emulsion are provided. The oil-in-water emulsion comprises an oil, a surfactant and an organic phosphate-based solvent. These methods can be used to inactivate a wide variety of bacteria such as Bacillus.
US7524949 Prevention or therapy of cardiovascular complications The present invention refers to inhibitors of the transcription factors IRF-1, their use as therapeutic agents as well as their use for prevention and therapy of cardiovascular complications like re-stenosis after percutaneous angioplasty or stenosis of venous bypasses, chronic (transplant arteriosclerosis or vasculopathy) or acute transplant rejection, graft versus host disease (GVHD), immunological hypersensitivity reactions (allergies), particularly bronchial asthma and atopic dermatitis, chronic recurrent inflammatory diseases, particularly ulcerative colitis and Crohn's disease, psoriasis and sarcoidosis, as well as autoimmune diseases, particularly diabetes mellitus, multiple sclerosis, collagenoses (e. g. systemic lupus erythematodes), rheumatoid arthritis and vasculotids.
CN101744835A Tungstenic compound nutriment for preventing and treating calculus and gout class diseases of urinary system The invention discloses a tungstenic compound nutriment for preventing and treating the calculus and the gout class diseases of the urinary system, which comprises at least one of tungstenic acid or salt, a tungstenic water soluble compound and tungstenic oxide. Tungsten in the tungstenic water soluble compound is +6 valence, +5 valence or +4 valence. The tungstenic oxide is tungstic oxide (WO3), tungsten pentoxide (W2O5) or tungsten dioxide (WO2). The tungstenic compound nutriment replaces or partially replaces clinically common used allopurinol in the treatment of the vesical calculus and the gout class diseases of the urinary system relevant to uric acid and salts thereof and overcomes the influence of the allopurinol on a human body because of influencing the relevant biochemical metabolism of xanthine oxidase, aldehyde oxidase and sulphite oxidase.
US20070027190 Antibacterial fab i inhibitors Disclosed herein are antibacterial compounds that inhibit fabl, a NADH-dependent enoyl [acyl carrier protein] reductase enzyme in the fatty acid biosynthesis pathway. The compounds are represented by structural formulas Ia and Ib: R1 and R2 are independently monocyclic aryl or heteroaryl groups, wherein the groups represented by R1 and R2 are optionally substituted with one or more acyclic substituents; R3 is —H or an optionally substituted C1-C8 aliphatic, C3-C8 cycloaliphatic, aryl, or heteroaryl group. X1 is a bond or a C1-C3 alkylene chain that is optionally substituted with a C1-C4 alkyl or an acidic group. X2 is an aryl, heteroaryl or C3-C8 cycloaliphatic ring, wherein the group represented by X2 is optionally substituted with triazole, tetrazole, and/or one or more acyclic substituents.
EP2084154A1 Aminoacyl prodrug derivatives and medicaments for treatment of thromboembolic disorders The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-l,3-oxazolidine-5-yl}methyl)thiophene-2-carboxamide, to processes for their preparation, to their use for treatment and/or prophylaxis of diseases and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.
EP1812418A1 Dibenzosuberone derivatives The present invention relates to compounds of formula (I), wherein R' and Rz are each independently hydrogen or halogen. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1, receptors.
DE102010049036A1 Aqueous solution, useful e.g. for rinsing tissues or organs of human or animal body, and for rinsing eyes or skin wounds, comprises sodium and potassium salts of mono hydrogen phosphate and dihydrogen phosphate Aqueous solution comprises sodium and potassium salts of mono hydrogen phosphate and dihydrogen phosphate, where the molar ratio of sodium to potassium is 24:1-40:1, the molar ratio of mono hydrogen phosphate to dihydrogen phosphate is 2:1-7:1, and the aqueous solution has a pH value of 7.2-7.6. - ACTIVITY : None given. - MECHANISM OF ACTION : None given.
WO2007046554A1 Process for production of dibenzoxepinopyrrole compound, intermediate for production of the compound, and process for production of the intermediate Disclosed is a process for production of a compound [VII] or a pharmacologically acceptable salt thereof, which comprises the steps of reacting a compound [III] with 4-chlorophenol to yield a compound [IV], subjecting the compound [IV] to an intramolecular ring closure reaction to yield a compound [V], reducing the compound [V] to yield a compound [VI], and reducing a carbonyl group in the compound [VI] to yield the desired compound [VII]. Also disclosed is an intermediate for the production of the compound [VII]. Further disclosed is a process for production of the intermediate.
CN101757493A Preparation method of epilepsy pills An epilepsy pill prepared by the invention has good efficacy, convenient taking, obvious effect and lasting efficacy for treating epilepsy.
WO2007095760A1 Cleavable carnitine compound The invention includes novel compounds, including but not limited to formula A and formula B, and an improved delivery method. These compounds and methods are useful in preventing or treating diseases or conditions associated with or caused by the presence of free radicals, and are useful for increasing cellular metabolism while simultaneously alleviating the resultant increase in oxidative stress. Specifically, a carnitine is bound to a lipoic acid derivative or to dihydrolipoic acid or its derivatives using a hydrolysable linker to form a single compound.
CN102885845A Application of Houttuynoid B in medicament for resisting tubercle bacillus The invention discloses an application of Houttuynoid B in the preparation of a medicament for resisting tubercle bacillus. Aiming at the current situation that the disease incidence and the mortality rate of tuberculosis have ascending trends due to high disease incidence of tuberculosis and the appearance of tubercle bacillus multiple drug-resistant strains at present, Houttuynoid B has the characteristic of obviously inhibiting the activity of tubercle bacillus and has good application prospect. The application of Houttuynoid B in the preparation of a medicament for resisting tubercle bacillus is firstly disclosed; since the skeleton type belongs to an entirely new skeleton type and the activity for inhibiting tubercle bacillus is previously unimagined high without any possibility of giving out revelation by other compounds, the application has outstanding substantial characteristics; and simultaneously, the application for preventing and treating tubercle bacillus infection is obviously advanced.
WO2013155739A1 Application of pigeon pea ketonic acid a in preparation of medicine for diabetes-accompanying disease and hyperlipidemia Application of the pigeon pea ketonic acid A and a pharmaceutically acceptable derivative thereof in preparation of a medicine for a diabetes-accompanying disease or hyperlipidemia as well as a functional health product. The diabetes-accompanying disease is hyperlipidemia, liver damage, kidney damage, or pancreas damage accompanying diabetes.
CN1981846A Enzyme inhibiting sprayable skin barrier compositions A skin barrier composition including a barrier component and an enzyme inhibiting component that is sprayable for use in ostomy and wound care, infant diapers, and fecal incontinence applications. The barrier component is based on petrolatum or other acceptable carriers, and the enzyme inhibitor component is derived from tubers, such as potatoes.
US20100215723 Wound Dressing with Antimicrobial Gauze and Bonding Agent A wound dressing (500) includes a flexible layer of material (501) that is treated with an antimicrobial agent (604), such as PHMB. The antimicrobial agent (604) ionically bonds to cellulose fibers (502) of the flexible layer of material (501) through a bonding agent (601). The bonding agent (601) increases the number of available carboxylate bonding groups beyond a characteristic carboxylate bonding group density normally associated with untreated cellulose fiber such that more antimicrobial agent (604) can be bonded to the flexible layer of material (501). An optional antifungal agent (606) can also be applied to the flexible layer of material (501).
US7183311 NF-κB inhibitors The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-β phosphorylation of IκB. In yso doing these aminothiophene inhibitors block pathological activation of transcription factor NF-κB in which diseases excessive activation of NF-κB is implicated.
CN101074233B 4'-demethylpodoph-yllotoxin derivative, its production and use A 4'-demethylepipodophyllotoxin derivative IIIa-n is prepared by taking etoposide as raw material, reacting with sodium iodide to generate 4-bit iodine substitute and obtain intermediate II, agitating while adding into barium carbonate, regulating reactive system pH 7-8, adding into amino-compound, and reacting to room temperature for 8-10 hrs to obtain final product. It's simple and efficient, it can avoid 4-bit surface isomerization and 4-bit demethylation, it has strong inhibiting function of multiple tumor cell strain and non-toxic.
WO2014059740A1 Tetracyclic anthraquinone derivatives Disclosed are a compound as shown in formula (I) and pharmaceutically acceptable salts thereof. R1, R2, R3, R4, R5, W, and n are defined as in the description of the present application.
WO2013054866A1 Agent for preventing or treating htlv-i associated myelopathy The present invention provides an agent for preventing or treating HAM and containing pentosan polysulfate or a pharmaceutically acceptable salt thereof as the active ingredient. The present invention also provides an agent for ameliorating HAM-associated motor disturbance and containing pentosan polysulfate or a pharmaceutically acceptable salt thereof as the active ingredient.
CN1729987A Cefuroxime sodium and sulbactam sodium composition for injection The invention provides a composition of cefuroxime sodium and sulbactam sodium for injection, which comprises cefuroxime sodium and sulbactam sodium by the weight ratio of 15:1. The composition has good antibiotic action and low cost of production.
WO2006015035A8 Useful compounds for hpv infection The present invention relates to compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.
CN101507821A Medicine for treating malignant cerebroma and breast cancer by combining gene and chemotherapy medicine and preparation method thereof The invention provides a medicine for jointly treating malignant cerebroma and breast cancer by combining gene therapy with chemotherapy, and a preparation method thereof. The medicine for jointly treating cell growth of cerebral gliomas and breast cancer is formed by taking polyamide-amine treelike molecules as a carrier and applying antisense mini RNA-21 genes combined with taxol as a chemotherapeutic drug. The preparation method comprises the following steps that: polyamide-amine is dissolved in a buffer solution and prepared into a solution A; as-miR-21 as a therapeutic gene is dissolved in the buffer solution and prepared into a solution B; the taxol is dissolved in a solution and prepared into a solution C; and the solution A and the solution B are mixed well and then added with the solution C at room temperature. Compared with the prior chemotherapy and individual gene therapy, combined medical treatment has the advantages of obviously strengthening the sensitivity of tumor cells to chemotherapeutic drugs, lowering the survival rate of the cells, increasing apoptosis percentage, obviously increasing the number of S-period cells, remarkably reducing the migration capability of the cells and inhibiting tumors more effectively.
US6884596 A compound that is a Prolactin Releasing Peptide receptor (PrRP) agonist; determining the ability of the compound to promote wakefulness; providing a PrRP receptor antagonist and determining the ability of the compound to promote sleep The invention provides methods of screening for a compound for promoting wakefulness in a mammal. The method is practiced by providing a compound that is a PrRP receptor agonist and determining the ability of the compound to promote wakefulness. Also provided by the invention are methods of screening for a compound for promoting sleep in a mammal. The methods are practiced by providing a compound that is a PrRP receptor antagonist and determining the ability of the compound to promote sleep. In addition, the invention provides a method of promoting wakefulness in a mammal. The method is practiced by administering to a mammal an effective amount of a PrRP receptor agonist. The invention further provides a method of promoting sleep in a mammal. The method is practiced by administering to a mammal an effective amount of a PrRP receptor antagonist.
EP2158907A2 A composition for use as a medicament for topical application to skin A delivery vehicle and method for delivering, either topically or orally, a nitric oxide releasing substance such as L-arginine 31 into human or mammalian tissue for the purpose of producing beneficial effects such as the relief of pain, the warming of cold tissues, the growth of hair on the scalp, the healing of leg ulcers, the relief of impotence as well as other beneficial effects. The delivery vehicle provides a hostile biophysical environment which facilitates and promotes the migration of the nitric oxide releasing substance into the tissue.
US20100254918 Agent for the prevention and treatment of the initial dental caries A composition for the prevention and treatment of initial tooth caries, that is composed of a phosphate-calcium gel with the Ca/P mass ratio ranging from 1.2 to 1.5 and with a bond energy of the 2p phosphorus electron of 131 eV to 136 eV and optionally containing at least one auxiliary dental substance. The composition can further contain an aqueous solution of methyl cellulose or/and chlorohexidine gluconate.
CN101011548A Medicine for treating ringworm of the nails and preparation method thereof The invention relates to a pharmaceutical composition for treating ringworm of the nails and process for preparation, wherein the composition is prepared from pangolin scales, musk, clove, banksia rose, Cinnamomum cassia, cortex pseudolaricis, flavescent sophora root, roor of sessile stemona, Chinese dittany bark, hydnocarpus seed, pricklyash peel, Chinese honey locust, cicada shell, dragon's bone, jack-in-the-pulpit tuber, pinellia tuber, Sichuan aconite root, Kusnezoff monkshood root, camphor, lead monoxide, Halitum Violaceoum, red lead, momordica seed, 2-hydroxybenzoic acid and benzene carboxylic acid through steps of powdering, heating, fermenting and mixing the powders with 2-hydroxybenzoic acid and benzene carbonic acid.
WO2007098860A1 New morphine compounds for pharmaceutical compositions The invention relates to new morphine compounds of the formula where R1 represents a C1-6 alkyl radical and the radicals R2 and R3 independently of one another are selected from the group consisting of hydrogen atoms, methyl groups and acetyl groups.
CN103565822A Application of hydrogen saturated physiological saline in preparing medicines for preventing and treating abdominal aortic aneurysm The invention relates to an application of hydrogen saturated physiological saline in preparing medicines for preventing and treating abdominal aortic aneurysm. Animal experiments show that the hydrogen saturated physiological saline through intraperitoneal injection not only can improve inflammatory cell infiltration and reduce inflammatory mediator release, but also can relieve tissue peroxidation and enhance antioxidant enzyme activities, so as to reduce expression of vascular wall proteolytic enzyme and inhibit degradation of vascular elastic fiber, thus relieving vascular injury, inhibiting angiectasis and reducing maximum outer diameter of blood vessel. The hydrogen physiological saline is simple in preparation process, convenient to use, low in cost, and free from toxic and side effects; animal experiments show that the hydrogen physiological saline has good advantages in prevention and treatment; therefore, the invention develops a new application of the hydrogen saturated physiological saline in preparing medicines for preventing and treating abdominal aortic aneurysm.
US20110243843 Fluorescent silica nanoparticles for detecting lymph node and the identification method of lymph node using thereof The present invention relates to fluorescent silica nanoparticles for detecting lymph node and identification method of lymph node using thereof. The functionalized silica nanoparticles containing fluorescent dye of this invention have a promising potential for sentinel node detection in the surgical field through fluorescent imaging.
CA2597910A1 Dosage form and method for sustained release of a substituted pyrazine compound The invention is directed to a dosage form and method for administering a therapeutic agent in a sustained release manner to provide an intended therapeutic effect while minimizing the side effects associated with the therapeutic agent. The therapeutic agent is selected from a group of substituted pyrazine compounds and may be (3)-(2,3,5-trichloro-phenyl)-pyrazine-(2,6)-diamine.
WO2011133795A2 Beta-carbolines as inhibitors of haspin and dyrk kinases The present disclosure is directed to compounds of Formula ( I ) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.
US20100280052 Use of antivirals to treat cmv-related conditions The invention provides for the use of compounds active against cytomegalovirus (CMV) in the preparation of medicaments for improving the immune response of a CMV-seropositive, immunocompetent individual, or for the amelioration of certain other medical conditions. Suitable compounds include the nucleoside analogues acyclovir, famciclovir, and valacyclovir. Infection with cytomegalovirus is widespread and commonly believed to be both asymptomatic in immunocompetent individuals and unbeatable without the use of highly cytotoxic drugs. It is suggested herein that, in fact, CMV infection produces a disproportionately large immune response, thereby weakening the ability of the immune system to respond to other infections (and hence is not asymptomatic). Further, treatment with comparatively low doses of drugs having low cytotoxicity (and hence similarly low efficacy) can reduce the magnitude of this CMV-specific immune response, improving the overall immune response, and ameliorating the symptoms of other medical conditions.
WO2012153870A1 Therapeutic material for glaucoma A therapeutic material for glaucoma, which is a kit comprising a laminate (A) that comprises an adhesive layer to be adhered to the surface of a biological tissue and a barrier layer, is biodegradable and contains no medicinal agent and a biodegradable matrix (B) that contains a medicinal agent, or which is a laminate comprising an adhesive layer (C) that is adhesive to the surface of a biological tissue, contains no medicinal agent and is biodegradable and a medicinal-agent-containing layer (D) that contains a medicinal agent and is biodegradable. When the therapeutic material for glaucoma is used, any scar of inflammation is not left around the sclera, a filtration bleb can be formed and maintained satisfactorily, there is not a problem of adverse side effects of mitomycin C, and the embrittlement of a conjunctival epithelial cell by a medicinal agent can be prevented.
CN1840060A Medicine for treating femoral head necrosis and femur head fracture and its preparation method The invention discloses a medicament for treating femoral head necrosis and neck of femur fracture, which is prepared from drynaria, linaloe, frankincense, myrrh, speranskia herb, Japanese yam, paris rhizome, keel, curculigo rhizome, dipsacus root, campeachy wood, sandalwood, Eupolyphaga Sinensis Walker, and dog's bone.
WO2013154513A1 The use of 5-ht7 receptor antagonists including some atypical antipsychotics as antipruritic agents The present invention is related to the role of 5-HT7 receptors in pruritus and using any pharmaceutical dosage forms containing therapeutically effective amount of 5-HT7 receptor antagonist including some atypical antipsychotics or drugs which modulate 5-HT7 receptors as alternative antipruritic agents. The any pharmaceutical dosage form containing 5-HT7 receptor antagonist including some atypical antipsychotics as an active ingredient are useful in relieving pruritus, complicated with some diseases, such as eczema atopic dermatitis, contact dermatitis, psoriasis, urticeria, sun burn, insect bites, contact with poisonous plants (e.g. poison ivy), biliary disease and jaundice, cholestasis, kidney disease, xeroderma, group of ichthyosis skin diseases, uremia, psychogenic itch such as delusional parasitosis, itching during pregnancy, hocfgkine lymphoma related itch, parasites and infections related itch, allergic conjuctivitis, thyroid disease related itch, diabetic itching and drug-induced pruritus as a side effect of medication.
CN101524362A Application of nucleic acid with CpG motif for preparing anti-fibrotic drug The invention discloses an application of nucleic acid with a CpG motif for preparing an anti-fibrosis drug. The invention provides a new application for the prior nucleic acid with the CpG motif, namely the preparation of the anti-fibrosis drug. The drug can prevent and reverse tissue fibrosis, in particular kidney fibrosis, lung fibrosis, cardiovascular tissue fibrosis and liver fibrosis. No effective drug and method exist for curing fibrosis diseases all the time, which chronically worries patients, family members and doctors of the diseases, such as chronic nephritis, high blood pressure, coronary heart diseases, chronic obstructive pulmonary diseases, liver cirrhosis, and the like. The nucleic acid with the CpG motif is acted on bacterins or curable small molecular substances for preventing and reversing the tissue fibrosis so as to effectively relief the pain of the patients and bring beneficial information for the health of human beings, thereby having wide curable prospects and important clinical meanings and social value.
WO2009007677A3 Dsb repair- inhibitors as anti-tumour agents There is provided a use of a DSB repair-inhibitor in the manufacture of a medicament for use in the treatment of a cancer in an individual, wherein the cancer comprises cells which are/is deficient in a BER and/or a SSBR pathway.
WO2011113855A2 Pharmaceutical composition for treatment of increased intraocular pressure The invention provides novel pharmaceutical compositions for the treatment of increased intraocular pressure based on semifluorinated alkanes which are useful as carriers for a broad range of active ingredients. Preferred active ingredients include poorly water-soluble prostaglandin analogues. The compositions can be administered topically into the eye. The invention further provides kits comprising such compositions.
WO2006109048A1 New tricyclic angiotensin ii agonists There is provided compounds of Formula (I), wherein A, X1, X2, X3, X4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceuticalfy-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
US20130041023 Composition for Preventing or Treating Rotavirus Infection Comprising Licorice Extract The present invention relates to a composition for preventing or treating rotavirus infection, comprising a licorice extract, fractions thereof or compounds separated therefrom. The licorice extract, fractions thereof or compounds separated therefrom have anti-rotavirus effects and exhibit not only virucidal effects against various rotaviruses, but also the effect of inhibiting the cytopathic effect of rotaviruses. Thus, the composition can be effectively used for the prevention or treatment of rotavirus infection.
CA2344308C Taurolidine and/or taurultam against infectious ulcer or gastritis A method for the treatment of infectious gastrointestinal ulcer disease or infectious gastritis disease of microbially infected gastrointestinal tissue in a mammal involves administration of an antimicrobial amount of an antimicrobial medicament which is cell wall constituent-inactivating by chemical reaction with cell wall constituents, endotoxin non-releasing, exotoxin-inactivating or a combination thereof.
US20100173009 Silicate-substituted hydroxyapatite An inorganic silicate-substituted calcium phosphate hydroxyapatite, useful as a biomaterial, has a Ca/P molar ratio in the range 2.05 to 2.55 and a Ca/(P+Si) molar ratio less than 1.66. The hydroxyapatite can be substantially free of carbonate ions. The material has relatively high solubility and is able to release silicon into solution.
CN103288807A Alkaloid separated from Tripterygium wilfordii endophytic fungus metabolite and application thereof The invention relates to an alkaloid separated from a Tripterygium wilfordii endophytic fungus metabolite and application thereof. The general formula of the alkaloid is shown in the specification, wherein R1 is -CH3 or -H; and R2 is one of -CH(CH3)2, -OH or -H. According to the invention, the alkaloid is separated from a Tripterygium wilfordii endophytic fungus metabolite for the first time, and the chemical structure of the alkaloid obtained by separation is determined, thus providing a realistic basis for the further study and practical application of Tripterygium wilfordii endophytic fungi.
CN103735549A Application of demethyleneberberine hydrochloride to preparation of medicament for treating nonalcoholic fatty liver disease The invention discloses application of demethyleneberberine hydrochloride as shown in a formula (I) to preparation of a medicament for treating the nonalcoholic fatty liver disease. The demethyleneberberine hydrochloride is shown in the formula (I) in the Specification.
EP2414348B1 Bicyclic piperidine and piperazine derivatives as gpcr modulators for the treatment of obesity, diabetes and other metabolic disorders The present invention relates to Bicyclic Piperidine and piperazine Derivatives, compositions comprising a Bicyclic Piperidine and piperazine Derivative, and methods of using the Bicyclic Piperidine and piperazine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
EP1256344B1 Remedies for endothelin-induced diseases Drug compositions for treatment of prostatic cancer, containing as the active ingredient N-[6-methoxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]-2-phenyl- ethenesulfonamide or pharmaceutically acceptable salts thereof.
US20090269328 Dry Composition for Oral Ingestion and Gel Composition Prepared Just Before Use for Oral Ingestion A dry composition for oral ingestion characterized by comprising as an active ingredient a gas-releasing substance which releases gas by soak with water, and further comprising a gel base in an amount sufficient for gel formation; a gel composition for oral ingestion formed by adding water or a liquid diluent to the dry compound when taking; and a mixed feed obtainable by mixing the gel composition with a feed, are disclosed.
US20090088477 Compounds and methods for leukotriene biosynthesis inhibition This invention provides novel salt and crystalline forms thereof of (−)4-(4-fluorophenyl)-7-[({5-[1-hydroxy-1-(trifluoromethyl)propyl]-1,3,4-oxadiazol-2-yl}amino)-methyl]-2H-chromen-2-one. The compounds are 5-LO inhibitors and are useful for treatment of conditions such as asthma, allergic rhinitis, COPD, and atherosclerosis.
CA2790602A1 10'-fluorinated vinca alkaloids provide enhanced biological activity against mdr cancer cells A 10'-fluoro-vinca alkaloid compound or its pharmaceutically acceptable salt is disclosed, as are methods of its preparation and use. A disclosed 10'-fluoro-vinca alkaloid compound has better cytotoxic potency against leukemia and cancer cell lines, and is about 8-times more cytotoxic to a multiple drug resistant cancer cell line than is a parental 10'-unsubstituted vinca alkaloid.
US7731983 Method and composition for the treatment of scars A method and composition for treating healed wounds including hypertrophic scars so as to prevent scarring or reduce the size and improve the appearance of scars comprises applying to the healed wound or scar a composition comprising a fluid, film-forming carrier which may contain one or more active topical ingredients, the carrier hardening to a solid, tangible, membrane juxtaposed to the skin. Novel compositions using the film-forming carrier are also useful to treat a variety of adverse skin disorders, and internal physiological conditions.
WO2010105930A1 Carbamate derivatives in particular for the treatment of neurological disorders The present invention relates to new carbamate derivatives of formula I, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders, such as neuropathic pain and anxiety.
EP1619962B1 Composition for oral administration containing capsaicinoids The invention concerns a composition for oral administration containing capsaicinoids associated with a formulation base acceptable for oral administration, said formulation base comprising an oil and an additive solid or pasty at room temperature which represents 5 to 20 wt. %, preferably 8 to 15 wt. % of the composition.
EP2014286A2 Cremophor free epothilone particles coated with protein for treating cancer In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful election of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within.
CN101874775A Revaprazan hydrochloride nanosuspension and preparation method thereof The invention discloses revaprazan hydrochloride nanosuspension and a preparation method thereof, belonging to the technical field of medicines. Revaprazan hydrochloride is a novel proton pump inhibitor and makes an effect of potentially inhibiting basal gastric acid secretion, but in-vivo bioavailability is low due to medicinal slight dissolution. By adopting a nano technology, the particle sizeof a medicine is reduced to prepare the nano-suspension and evaluate the in-vitro dissolution and the in-vivo bioavailability of the nano-suspension of the medicine. A determining result shows that the nano-suspension can greatly improve the dissolution and the bioavailability of the medicine. The invention further discloses the preparation method of the nano-suspension.
CN103159735A Substitutional imidazole kinase inhibitor The invention belongs to the field of medical technology, in particular to a substitutional imidazole kinase inhibitor which is shown by general formulas (I), (II), salt or a stereoisomer which are acceptable in pharmacy, wherein, R1, R2, R3, L1 and L2 are defined the same as the definitions in an instruction book. The invention further relates to preparation methods of the compounds, pharmaceutic preparation and pharmaceutical compositions which include the compounds, the compounds, and the application of the compounds, the salt or the stereoisomer which are acceptable in pharmacy in the drugs of preparing, treating and/or preventing diseases which are related to or not related to cancers caused by mutation of b-RAF.
WO2009022064A3 Novel naphthalene derivatives, process for the preparation thereof and pharmaceutical compositions containing same Compounds of formula (I): in which: R1 is alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, and R2 is a fluorine atom or an alkyl group substituted with one or more fluorine atoms. Medicaments.
CN101502524B Application of acetyl-fluorobenzene salicylamide compound in preparing anti-tumor medicament The invention discloses the application of acetyl fluorobenzene salicylamide type compounds as shown in formula (I-1) to formula (I-7) in the preparation of anti-tumor drugs. The invention provides a novel anti-tumor drug having significant anti-tumor activity and provides the foundation for the research of drug-screening, wherein, the compound as shown in formula (I-1), formula (I-6) or formula (I-7) has very significant anti-tumor effect; the compound as shown in formula (I-3) or formula (I-4) has significant anti-tumor effect; the compound as shown in formula (I-5) has relatively good anti-tumor effect; and the compound as shown in formula (I-2) has certain anti-tumor effect.
US20110014308 Novel compositions and use thereof for the treatment, co-treatment or prevention of inflammatory disorders. The present invention relates to novel compositions comprising hydroxytyrosol and chondroitin as well as to the use of these compositions as a medicament, in particular as a medicament for the treatment, co-treatment or prevention of inflammatory disorders.
WO2007147330A1 The application of the bakuchiol compounds The application of the bakuchiol compounds in the preparation of a medicament for treating the psychopathy or the neuropathy. The bakuchiol compounds can selectively inhibit the activity of the dopamine transport protein, the norepinephrine transport protein and the 5-HT transport protein, whereas have no influence on the activity of the Ϝ-propalanine transport protein and the L-glutamic acid and have no cytotoxicity.
US20080153868 Substituted Tetrahydroisoquinolines as Beta-secretase Inhibitors There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
EP1618090A1 11ß-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS A novel class of compounds of the general formula (I) in which R1 and R2 form a saturated or partially saturated bicyclic or tricyclic ring system, their use in therapy, pharma-ceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of dis-eases in which such a modulation is beneficial, e.g. the metabolic syndrome.
US20100196316 Cyclosporin analogues for preventing or treating hepatitis c infection The present invention relates to cyclosporin analogues having antiviral activity against HCV and useful in the treatment of HCV infections. More particularly, the invention relates to novel cyclosporin analogue compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.
US20080182824 e.g. N-methyl-N-propargyl-4-hydroxybenzyl amine; monoamine oxidase inhibitors; are mediated via a peripheral (i.e., non-CNS) mechanism; antidiabetic agent, metabolic disordes, obesity, insulin resistance The invention provides novel N-benzyl-N-propargyl-amines that are monoamine oxidase inhibitors, but generally exhibit little or no CNS effects.
US20090082441 Deuterium-enriched tesaglitazar The present application describes deuterium-enriched tesaglitazar, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2006037185A1 Novel sulfenamides and sulfenamide oxides A compound of the general formula (I): wherein R1, R2, X1, X1', X2, X2', X3, X3', X4, X4' and X5 define various substituents and p is 0, 1 or 2. The invention also relates to use of the compounds as anti-microbial agents.
US20090143295 Peptide-based antiacne reagents Peptide-based antiacne reagents, formed by coupling a skin-binding peptide with an antiacne agent, are described. The skin-binding peptide portion of the peptide-based antiacne reagent binds strongly to the skin, thus keeping the antiacne agent coupled to the skin for a long lasting effect. Skin care compositions comprising the peptide-based antiacne reagents are also provided as well as a method of treating or preventing skin acne.
US20130195960 Substituted Cellulose Acetates and Uses Thereof The present invention relates to substituted cellulose acetates and methods of use thereof. One embodiment of the present invention provides a diaper having an inner layer having an absorbent core having a substituted cellulose acetate having a polar substituent that has an oxygen atom covalently bonded to a nonmetal selected from the group of sulfur, phosphorus, boron, and chlorine; wherein the nonmetal is present in at least about 0.01% by weight of the substituted cellulose acetate; and an outer layer.
WO2010072950A1 Formulation for delivering lipid-lowering drugs by oral transmucosal administration The invention relates to a formulation for delivering at least one lipid-lowering active principle by oral transmucosal administration, preferably of the statin family, said formulation including said active principle in the form of a base or a salt, a hydroalcoholic solution containing water and ethanol with an alcoholic content of at least 30% ABW, and optionally a pH correcting agent and/or an anti-oxidiser, said active principle being at a stable and complete dissolution state in the hydroalcoholic solution. The invention also relates to a method for preparing said formulation and to the use thereof, preferably in a single-dose packaging, for treating and preventing hyperlipemia and/or cardiovascular disorders.
US8158681 Nutraceutical and pharmaceutical compositions and use thereof for the treatment, co-treatment or prevention of inflammatory disorders The present invention relates to new methoxylated aromatic compounds. It also relates to novel compositions comprising methoxylated aromatic compounds as well as to the use of these compositions as a medicament, in particular as a medicament for the treatment, co-treatment or prevention of inflammatory disorders.
CN102824348A New technology for extracting sterol from corn germ oil deodorization distillate The invention discloses a technology for extracting sterol from a corn germ oil deodorization distillate. The technology comprises the following steps: adding methanol to the corn germ oil deodorization distillate which is a raw material, converting free fatty acids in the raw material into corresponding methyl esters with a strong-acidic cation exchange resin as a catalyst, carrying out cold separation to extract crude sterol, and decoloring; and 2, re-crystallizing through adopting a mixed solvent of ethanol and n-hexane having a volume equal to the volume of the ethanol in the crystallization process to purify the crude sterol. The invention discloses a preparation method of a sterol-cyclodextrin inclusion compound to improve the utilization value of the sterol. The preparation method comprises the following steps: adding fully-dried sterol to a water-free solvent having a temperature of 25-85DEG C, dissolving, adding a solubilizer to dissolve, stirring at 30-100r/m for 2-20h, cooling to 0-4DEG C, maintaining the temperature until crystals fully precipitate, filtering, and separating the crystals from a crystallization mother solution, wherein the crystals are the sterol-cyclodextrin inclusion compound.
EP2415869A1 Modified oligo-nucleic acid molecule, preparation method and uses thereof The present invention relates to a modified oligonucleotide, its preparation and application. The invention eables stabilizing the oligonucleotide by introducing a relatively small amount of modified nucleotide at specific UA/UA and/or CA/UG and/or UG/CA site of the oligonucleotide, therefore to decrease the modification-related cytotoxicity and compromising effects on the biological activity.
EP1330254B1 Treatment of cancers by aplidine in conjunction with carnitine or acetylcarnitine Carnitine and other muscle protectors are useful to prevent side effects of aplidine and aplidine analogues.
WO2008064132A3 Synthetic triterpenoids and tricyclic-bis-enones for use in stimulating bone and cartilage growth The present invention concerns methods for stimulating the growth and repair of bone and cartilage using synthetic triterpenoids and tricyclic-bis-enones. Examples of suitable triterpenoids include CDDO, CDDO-Me, CDDO-Im, and CDDO- Ethylamide. Examples of tricyclic-bis-enones include TBE-31 and TBE-34.
WO2008137787A2 Combination therapy with a compound acting as a platelet adp receptor inhibitor The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing [4 (6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, for the treatment of thrombosis diseases.
US20100137274 Rivaroxaban and derivatives, synthesis; atherosclerosis; arthritis; Alzheimer's disease or cancer The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
US20110184220 Methods for the treatment of radiation or chemotherapy-induced tissue damage The present invention relates to methods for preventing or treating toxicities associated with exposure to ionizing radiation or to chemotherapy. Particularly, the present invention relates to methods for preventing or treating toxicities associated with radiation or chemotherapy comprising administering to a subject in need of such treatment polypeptide complexes comprising an IL-6 linked to a soluble IL-6 receptor, the polypeptide complexes capable of preventing or treating toxicities, particularly xerostomia.
US7144918 Enzyme inhibitors; anticancer agents The present invention provides a compound of the formula (I). The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.
US7845348 Methods for treating trigeminal neuralgia Apparatus, methods, and kits for treating symptoms associated with common ailments, such as headaches, rhinitis, asthma, epilepsy, nervous disorders and the like, are provided. The apparatus comprises dispensers for carbon dioxide and other therapeutic gases. The methods comprise delivering small volumes of these gases to patients in a manner where the gas infuses into a body region in order to bathe the mucous membranes therein. It has been found that even very short exposure of patients to small volumes and high concentrations of such gases can provide significant relief from symptoms.
EP0938476B1 Process for substituted pyridines This invention relates to processes for preparing compounds of formula (I) which are β-adrenergic receptor agonists, and to processes for preparing certain intermediates of formula (IIA) wherein R1 is nitro, amino or protected amino; R2 is H, fluoro, chloro CF¿3?, nitro, (C1-C4)alkyl, (C1-C4)alkoxy, amino or protected amino; and X?1¿ is OH or a suitable leaving group, used in that process. The invention also relates to novel compounds of the formulae (II).
US20080058284 Pharmaceutical compositions of semicarbazones and/or thiosemicarbazones and/or their derivatives and products of these compositions and their uses as anticonvulsant, anti-nociceptive and anti-inflammatory agents, and in the angiogenic therapy The present invention is characterized by obtaining inclusion compounds of semicarbazones and/or thiosemicarbazones and/or their derivatives in cyclodextrins and/or their derivatives, which once tested in experimental models of epilepsia allowed the reduction of anticonvulsant dose from 100 mg/kg to 25 mg/kg. This means an increase in bioavailability of compounds in biological systems. Hence inclusion compounds between semicarbazones and/or thiosemicarbazones and cyclodextrins and their derivatives could be new candidates as anticonvulsant agents. The present invention is also characterized by the increase in the anticonvulsant efficacy of the inclusion compounds between cyclodextrins and/or their derivatives and semicarbazones and/or thiosemicarbazones and/or their derivatives in comparison to free components.
US20060135588 Preventive and/or therapeutic drugs for inflammatory intestinal diseases The object of the present invention is to provide a medicament useful for preventing and/or treating inflammatory bowel disease. The present invention provides a medicament for preventing and/or treating inflammatory bowel disease which comprises as an active ingredient a pyrazolone derivative represented by the following formula (I) or a physiologically acceptable salt thereof, or a hydrate thereof or a solvate thereof: wherein R1 represents a hydrogen atom, an aryl group, an alkyl group, or an alkoxycarbonylalkyl group; R2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group or a hydroxyalkyl group; or R1 and R2 are combined with each other to represent an alkylene group; and R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, a benzyl group, a naphthyl group, a phenyl group, or a phenyl group substituted with 1 to 3 substituents selected from the group consisting of an alkyl group, an alkoxy group, a hydroxyalkyl group, an alkoxycarbonyl group, an alkylmercapto group, an alkylamino group, a dialkylamino group, a halogen atom, a trifluoromethyl group, a carboxyl group, a cyano group, a hydroxyl group, a nitro group, an amino group and an acetamide group.
EP0901372B1 Potassium, sodium and tris oxaprozin salt pharmaceutical formulations The present invention provides a pharmaceutical formulation for oral administration which is pharmaceutically acceptable, and which produces a desired therapeutic response, in tablet, caplet or other compressed form which comprises the potassium, sodium or Tris salt of oxaprozin, the tablet, caplet or other compressed form of the pharmaceutical formulation generally becoming about 75 % dissolved in phosphate buffer media within about 30 minutes.
US20100130552 Therapeutic Agents Useful for Treating Pain A compound of Formula: (I) or a pharmaceutically acceptable derivative thereof, where Ar1, Ar2, X, R3, and m are as disclosed herein. Compounds of Formulae (I)-(V) and pharmaceutically acceptable derivatives thereof; compositions comprising an effective amount of a compound of Formulae (I)-(V) or a pharmaceutically acceptable derivative thereof; and methods for treating or preventing pain, UI, an ulcer, IBD, or IBS in an animal comprising administering to an animal in need thereof an effective amount of a compound of Formulae (I)-(V) or a pharmaceutically acceptable derivative thereof are disclosed herein.
US20080248012 Modulator of adenosine triphosphate release from red blood cells; treating and preventing ischemic reperfusion injuries, cardiovascular and vasodilatory diseases A promoter of ATP release from red blood cells, comprising a substance capable of stabilizing the structure of hemoglobin in red blood cells in its T-state; and a method of releasing ATP from red blood cells with the use of the promoter. There are further provided an inhibitor of ATP release from red blood cells, comprising a substance capable of stabilizing the structure of hemoglobin in red blood cells in its R-state; and a method of inhibiting ATP release from red blood cells with the use of the inhibitor.
CN101591348A Tetrahydrochysene carboline acyl aminoacid benzyl ester, preparation method and application thereof The invention discloses a general formula I compound with antitumor activity, a preparation method and application thereof, belonging to the biomedicine field. The invention adopts an S180 mouse model to evaluate the antitumor activity of the compound 8a-s. Experimental results show that the compound of the invention has excellent antitumor activity and can be clinically applied as the antitumor agent.
CN1969882A Sugar-free vitamin oral liquid Disclosed is a sugar-free vitamin oral liquid, wherein each 1ml comprises the following constituents: vitamin 1500-3500 international units, vitamin D 400-600 international units, vitamin E 1-5mg, vitamin B1 0.5-2.5mg, vitamin B2 0.5-2.5mg, vitamin B6 0.5-2.5mg, vitamin B12 0.5-6ug, vitamin C 35-70mg, vitamin K1 10-25ug, biotin 10-30ug, and folic acid 40-400ug, nicotinamide 6-20mg and pantothenic acid 5-10mg.
US7033617 Use of Anoectochilus formosanus plant extracts and their derived fractions as herbal medicines or nutraceutical supplements for chemoprevention or treatment of human malignancies The present invention provides medicinally active extracts and fractions, and a method for preparing the same by extracting and fractioning constituents from the tissue of plant components of the Anoectochilus family. These active extracts and fractions are useful for preventing or inhibiting tumor growth.
CN103649086A Methods for preparing naphthyridines The present invention provides methods of synthesizing compounds of formula (1) and intermediates thereto. The present invention also provides intermediates useful in the synthesis of compounds of formula (1).
CN101007804A 1,3-benzodioxole-2,2-dicarboxylic acid derivatives and their preparation method and medicinal uses The invention relates to compound in general formula I, comprising its racemic or optical isomer, or salt accepted by pharmacy or solvate. The definition of each substituent group is expressed in claims. The invention also relates to the method for preparing said compoundin in general formula I and the its application in preparing medicine for treating and/ or preventing diseases relevant to human hyperoxide enzyme propagation factor activation reacptor (hPPAR).
CN101317943A Medicament for treating periodontitis and preparation thereof A medicine for curing peridentitis is characterized in that the medicine contains dry zanthoxylum pericarp, garlic and mature vinegar and the weight percentage range of the raw materials is 1-2:15-25-74-84. During preparation, garlic is peeled and immersed in mature vinegar for 8 to 12 days; then after adding dry zanthoxylum pericarp, garlic is immersed in mature vinegar for another 20 to 25 hours. The medicine for curing peridentitis provided by the present invention has the advantages of rapid effect, low cost and easy operation.
CN1868498A Gutweed total flavone, its prepn. method, freeze-drying powder injection containing it and quality control method therefor A general ixeris flavone containing luteolin-7-0-beta-D-phranoglucuronide (C21H18O12), a freeze-dried powder injection prepared from said general ixeris flavone, mannitol and the water for injection, and the preparing process and quality control method of said freeze-dried powder injection are disclosed.
US20120214779 Application of 20(s)-protopanaxadiol in preparation of antidepressants The invention provides the novel use of 20(S)-protopanaxadiol in the preparation of medicaments for the treatment of depressive psychiatric disorders. The pharmacological test results indicated that the compound could remarkably increase the level of NE, 5-HT and HAV in the brains of model rats having depressive disorders, remarkably enhance tremors induced by 5-hydroxytryptophan (5-HTP) and behavioral effects induced by levodopa, and inhibit the re-uptake of 5-HT and NA.
CN101255178A C-glycoside and C-glycoside compound containing substituted aromatic rings as well as preparation and use thereofb The invention discloses C-glycoside with substituted aromatic ring, S-glycoside compounds, pharmaceutical compositions with effective dose compounds, and applications of the compounds and compositions for preparing cardio-cerebrovascular anti-hypoxic ischemia medicine and neuroprotection medicine. In the compounds are c-glycoside compounds when X represents CH2, wherein when Y represents CH2, n may be 0 or 1, when n is 0, m is 0, and when n is 1, m is 0 or 1; when Y represents NH, n=m=1; when X represents S, the compounds is S-glycoside compounds, wherein Y represents CH2, n may be 1, 2 or 3, and m is 0; R represents mono-substituted, disubstituted, tri-substituted hydrogen C1-C3 straight-chain or branched chain alkyl and hydroxyl, or C1-C3 straight-chain or carboxylic acid ester. 14 compounds found have better protective action to hypoxia-reoxygenation injury of myocardium than or equal to salidroside; 15 compounds have stronger neuroprotection activity than or equal to gastrodine.
CN103232520A Spirosteroid compounds and preparation method and medical application thereof The invention relates to the field of biomedicines, and in particular relates to spirosteroid compounds shown as formula I-VII or pharmaceutically acceptable salts and officinal carriers thereof, a preparation method of the spirosteroid compounds or pharmaceutically acceptable salts and officinal carriers thereof, an officinal composition comprising the compounds and medical application of the spirosteroid compounds or pharmaceutically acceptable salts and officinal carriers thereof. Pharmacological experiment results show that the compounds have good anti-inflammatory and anti-tumor activities and are clinically used to prepare medicines for treating inflammatory diseases and tumors.
CN103462906A Injection docetaxel nanoparticle and preparation method thereof The invention discloses an injection docetaxel nanoparticle and a preparation method of the injection docetaxel nanoparticle. The preparation method comprises the steps as follows: mixing oil phase and water phase, homogenating with a high-speed homogenizer, homogenizing with a high-pressure homogenizer, adding the obtained nanoemulsion into a freeze-drying stent agent after homogenizing, removing an organic solvent with a rotary evaporator, concentrating, filtering, and conducting freeze-drying to prepare the injection freeze-drying nanoparticle with good stability and low toxic and side effects and with the particle size within the range of 10-100nm. The preparation method provided by the invention is simple and easy to operate, the water solubility is high, the dispersibility is good, and the toxic and side effects caused by using Tween 80 as a solubilizer are avoided. The nanoparticle prepared with the method wraps the docetaxel in lipidosome to prepare the O/W lipid nanoparticle. The solubility of the medicine is increased, the retention time of the docetaxel in the body is prolonged, and the toxic and side effects of the docetaxel as a common injection are reduced.
US20110195928 Administration of Copper to an Animal The present invention is directed to the administration of copper to an animal using a composition containing copper dextran. A method is described for increasing the copper levels in an animal by the administration of a composition containing copper dextran. A preferred method of administration is intra muscularly. The use of this composition has been found to both address copper deficiencies in an animal, particularly deer.
US20090318388 Method of activation of oxazaphosphorines The present invention provides a method of hydroxylating or oxidizing a compound of interest in a subject (e.g., a cytotoxic oxazaphosphorine prodrug), by administering the compound of interest to the subject; and concurrently administering the subject a metalloporphyrin in an amount effective to hydroxylate or oxidize the compound of interest in the subject.
CN101829098A Application of substituted isosilybin in preparing medicament for treating virus hepatitis B The invention relates to application of substituted isosilybin in preparing a medicament for treating virus hepatitis B, in particular to application of E-ring substituted isosilybin or medicinal salt thereof in preparing a medicament for clearing hepatitis B e antigen, inhibiting HBV DNA replication and treating hepatitis B virus infected diseases. The E-ring substituted isosilybin has strong effect of inhibiting HBeAg activity, and the strength of the E-ring substituted isosilybin at the concentration of 100 micrograms per milliliter for clearing the HBeAg is 3.5 times that of a positive control front-line medicament (10,000 units per milliliter of alpha-interferon); and moreover, the compound at the concentration of 100 micrograms per milliliter has strong inhibiting rate (97.7 percent) on the HBV DNA. Pharmacodynamical results show that the E-ring substituted isosilybin or the medicinal salt thereof can be expected to be used for preparing the medicament for treating the hepatitis B virus infected diseases.
CN103724310A Bavachinin C-ring carbonyl reduction product and biological preparation method thereof The invention relates to a bavachinin C-ring carbonyl reduction product and a biological preparation method thereof. The method comprises the following steps: carrying out conversion reaction by taking bavachinin as a substrate, adopting penicillium raistrickii ATCC 10490 as a biocatalyst, and carrying out organic solvent extraction and silica gel separation and purification so as to obtain derivatives of the bavachinin C-ring carbonyl reduction product. The method is simple in technological step, high in safety, and efficient and specific in reaction. By adopting the method, the problems that the existing chemical preparation method of flavanone compound derivatives is low in reaction efficiency, a lot of organic solvents are utilized, the product is difficult to separate and purify, and the like are overcome; the prepared bavachinin C-ring carbonyl reduction product is a novel compound with a novel structure; the bavachinin C-ring carbonyl reduction product has a certain proliferation acceleration effect on normal cells, and has anti-tumor activity which is equivalent to or better than that of the substrate.
CN100581548C Citric acid Mosabily oral liquid An orally taken solution of mosapride citrate is prepared from mosapride citrate, glycerin, alcohol, propanediol, polyethanediol-300, polyethanediol-400, antisetic and flavouring. It has fast absorption rate and high stability.
CA2265993C Novel antimicrobial cosmetic compositions The present invention relates to cosmetic or pharmaceutical formulations for topical application which comprises an antimicrobial effective amount of 3-furan carboxylic acid. The formulation also optionally comprises an anti-irritant effective amount of ferulic acid and an antimicrobial effective amount of 2-furan carboxylic acid. The invention also provides cosmetic or pharmaceutical compositions useful in the treatment of inflammation, comprising effective amounts of 2-furan carboxylic acid or 3-furan carboxylic acid, or mixtures thereof.
WO2006000421A2 Ige antibody repressing agent comprising alpha cyclodextrin The present invention provides a safe IgE antibody repressing agent and foodstuff of high therapeutical effect. This IgE antibody repressing agent and foodstuff efficient in improving IgE allergic diseases comprises alpha-cyclodextrin as an active component.
US20110280964 Composition And Method of Treating Hearing Loss A composition for treating hearing loss includes components that function through different biological mechanisms to provide an additive effect that is equal to or greater than a sum of the effect of the individual components. The composition includes a biologically effective amount of at least one scavenger of singlet oxygen, a donor antioxidant, a third antioxidant, and a vasodilator. A method of treating hearing loss includes the step of internally administering the composition including a biologically effective amount of the at least one scavenger of singlet oxygen, the donor antioxidant, the third antioxidant, and the vasodilator to a mammal within three days of trauma to a middle or inner ear of the mammal.
US20110009456 Compounds, Compositions and Methods for Treatment and Prevention of Orthopoxvirus Infections and Associated Diseases Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.
CN102525936A Compound epirubicin hydrochloride polylactic-co-glycolic acid (PLGA) nanoparticles and preparation method thereof The invention relates to a compound anti-tumor nanoparticle preparation and a production technology thereof, in particular to a compound epirubicin hydrochloride polylactic-co-glycolic acid (PLGA) nanoparticles and a preparation method thereof. In order to overcome the defects that the in vivo retention time of epirubicin hydrochloride and gadopentetate dimeglumine is short and the treatment effect is inconvenient to observe, the epirubicin hydrochloride and the gadopentetate dimeglumine are used together to prepare the compound nanoparticle preparation containing the epirubicin hydrochloride and the gadopentetate dimeglumine, so that the medicine can stay at the tumor position for a long time and release, and the anti-tumor effect can be detected in real time. The therapeutic medicine with the detection function has wide clinical application prospect. Due to the compound epirubicin hydrochloride nanoparticles, a basis is laid for application of the nanoparticle preparation with the detection medicine to clinical treatment on liver cancer and the like.
WO2009041765A1 Pharmaceutical composition containing esomeprazole The present invention relates to esomeprazole free base or its alkali salt-containing composition which stability is improved and is easy to manufacture.
US20120015897 Novel formulation for treating fungal infections A novel formulation for treating fungal infections comprising Cholesterol containing Nanosomal Amphotericin B in a Saline Suspension
WO2012044572A1 Dual inhibitors of met and vegf for the treatment of castration- resistant prostate cancer and osteoblastic bone metastases This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.
EP2141994A1 Multi-ring compounds and uses thereof Chemical agents, such as derivatives of hydroxy benzene moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
EP1414500A4 Akt and regulation of ra synovial fibroblast apoptosis The administration of an Akt inhibitor in a suitable carrier to a rheumatoid arthritis synovial fibroblast affords a process for inducing rheumatoid arthritis synovial fibroblast apoptosis. The Akt inhibitor is administered either as an active molecule or as a gene sequence expressible within rheumatoid arthritis synovial fibroblast cells. The gene sequence can be encompassed within a gene vector such as an adenovirus. A process for assaying rheumatoid arthritis drug candidates for apoptosis affect includes exposing a culture of rheumatoid arthritis synovial fibroblast cells to a drug candidate and monitoring apoptosis in the culture in the presence of the drug candidate. Apoptosis in the culture is compared to apoptosis induced in a duplicate culture in the presence of a known Akt inhibitor.
CN102552360A Composition for treating tumor The invention provides a composition for treating a tumor, which takes bighead atractylodes rhizome volatile oil and muscone as medicinal effective components, wherein the mass ratio of the bighead atractylodes rhizome volatile oil to the muscone is 1: (10000-100000). The composition for treating the tumor is obtained by doping trace amount of the muscone into the bighead atractylodes rhizome volatile oil, and the muscone and the bighead atractylodes rhizome volatile oil have the synergistic effect; an experiment shows that the addition of the muscone greatly improves the anti-tumor effect ofbighead atractylodes rhizome essential oil; the treating effect of the composition on the tumor is greatly improved compared with the treating effect of only using the bighead atractylodes rhizome volatile oil, and the effect is obvious; and the composition provided by the invention is simple in preparation process and needed equipment, so that the composition is good for production in a large scale.
WO2013096577A1 Antimicrobial composition for animal welfare An antimicrobial solution for disinfecting or removing micro-organisms from a surface used by animals or for use as an animal shampoo is described. The solution is active against bacteria, fungi, and viruses, including enveloped viruses, and skin disorders related to insect infestation.
WO2008031221A1 Isovaline for treatment of pain The invention provides for the use of isovaline or a pharmaceutically acceptable salt thereof for the treatment of Pain in a mammalian subject in some preferred embodiments, the invention provides for the treatment of acute and chronic Pain syndromes where other drug therapies have limited efficacy or unacceptable toxicity in said subject.
CN102885761A Method for preparing tacrolimus ointment The invention provides a method for preparing a tacrolimus ointment. The method comprises the following steps of: 1, weighing purified tacrolimus, white beeswax, liquid paraffin, paraffin, white Vaseline, propene carbonate and propanediol in the mass ratio of 1:30:40:30:520:10:10; 2, mixing the white beeswax with the liquid paraffin and the paraffin, heating for melting, mixing uniformly to obtain a mixed solution I, and preserving heat at the temperature of 70 DEG C for later use; 3, heating white Vaseline for melting to obtain a white Vaseline solution, and preserving heat at the temperature of 70 DEG C for later use; 4, mixing propanediol and propene carbonate uniformly in the ratio of 1:1 to obtain a mixed solution 2; 5, dissolving tacrolimus into the mixed solution of propanediol and propene carbonate to obtain a mixed solution 3, and preserving heat at the temperature of 70 DEG C for later use; and 6, dispersing the mixed solution 3 into the white Vaseline solution to obtain a mixed solution 4, adding the mixed solution 4 into the mixed solution I to obtain a solution 5, stirring at the temperature of 70 DEG C for 10 minutes, cooling, and continually stirring till the solution 5 is condensed into an ointment.
CN101732267A Pravastatin sodium tablet as well as application and preparation method thereof The invention provides a pravastatin sodium tablet as well as application and a preparation method thereof. The pravastatin sodium tablet contains pravastatin sodium, mannitol as filler, a basifier, a caking agent and a lubricating agent. The pravastatin sodium tablet is prepared by using a direct tablet compressing method, has higher stability and is beneficial to the storage and the transportation of medicines.
US20120093948 Nitric Oxide Treatments Portable and pure nitric oxide delivery systems can be used to treat a variety of patient conditions.
US7041316 Stable oral pharmaceutical dosage forms The present invention relates to new stable enteric coated pharmaceutical dosage forms for oral use containing Omeprazole or Lansoprazole, to a formulation and a method for the manufacture of such a dosage forms, and to a method of gastric acid pump inhibition and providing gastrointestinal cytoprotective benefit by using them.
US20100010072 Microrna biomarkers for human breast and lung cancer The present invention relates to novel molecular markers for diagnosis and classification of human breast cancer and lung cancer.
CN101095686A Method for producing lecithin capsule, lin ester alcohols and lecithin oral liquid The invention provides processes for preparing lecithin capsule, phosphatidic acid and lecithin oral liquid. The lecithin capsule is prepared from medicinal lecithin, VE, VC, lycine, methionine, olive oil and salad oil through mixing, stirring, forming, sterilizing and disinfecting. Phosphatidic acid is prepared from medicinal lecithin, epimeddium, astragalus root, schisandra fruit and wolferry fruit through white spirit immersing and filtering. Lecithin oral liquid is prepared from medicinal lecithin, wheat germ, carrot extract, laevulose, thickening agent and water through immersing and boiling wheat germ in water, filtering, charging other components into the liquor, homogenizing and loading, sterilizing and disinfecting.
CA2703720A1 Improved antitumoral treatments The present invention relates to combinations of PM02734 with EGFR tyrosine kinase inhibitors, and the use of these combinations in the treatment of cancer.
WO2008148801A3 Disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission The present invention relates to the use of compounds which increase extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically to the use of 3-disubstituted phenyl-1 - pyrrolidinols for the treatment of central nervous system disorders.
CN101879183A Diabetes mellitus treatment medicament formed by matching alpha-ricinoleic acid ethyl ester with chitosan The invention discloses a diabetes mellitus treatment medicament formed by matching alpha-ricinoleic acid ethyl ester with chitosan and a preparation method thereof and also relates to application of the medicament for treating the diabetes mellitus and effectively improving complications which are easily caused by the diabetes mellitus. The diabetes mellitus treatment medicament is formed by matching the alpha-ricinoleic acid ethyl ester with the chitosan, wherein the weight ratio of the alpha-ricinoleic acid ethyl ester to the chitosan is 0.1-1:1; the content of alpha-ricinoleic acid in the alpha-ricinoleic acid ethyl ester is more than or equal to 70 percent; and the consumption of the chitosan is 1-5g/person/day. The invention is used as the medicament or food for treating and preventing the diabetes mellitus and diseases relevant with the diabetes mellitus, wherein the main substance of the alpha-ricinoleic acid is a fundamental substance for forming brain cells, tissue cell membrane and biological enzyme of human body and can promote the insulin secretion and reduce the resistance on insulin; and in addition, the protection function and the enhancement function of the alpha-ricinoleic acid on various organs and a nervous system of human body are greatly beneficial for diabetics to prevent the complications.
US20100069390 Method of treatment of attention deficit/hyperactivity disorder (ADHD) The invention comprises a method for treatment of ADHD or ADHD-related disorders by a pharmaceutical agent exhibiting combined serotonergic or noradrenergic reuptake transporters and monoamine receptor activity.
US6861429 2,3-diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2 (COX-2) inhibitors The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, ester or salt or solvate of such ester, of a compound of formula (I) in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H and C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4; and a sodium channel inhibitor.
US7256218 Biguanide and dihydrotriazine derivatives Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.
CN103536935A Photosensitizer-modified core-shell structure magnetic nanocomposites and preparation method and application thereof The invention belongs to the field of nanocomposites and particularly relates to photosensitizer-modified core-shell structure magnetic nanocomposites, and a preparation method and application thereof. Manganous-manganic oxide nano particles with oil solubility are prepared by a solvothermal method; the manganous-manganic oxide nano particles with oil solubility are subjected to water-soluble modification and then are coated with mesoporous silica by a sol-gel method; and amino-functionalization is carried out, so that a lot of amidogens can be combined with photosensitizer molecules Ce6 on the surface. The nanometer materials are uniform in grain size which is about 60nm, have good dispersibility, excellent biocompatibility and good T1 weighted imaging effect. The photosensitizer-modified core-shell structure magnetic nanocomposites can be applied to preparation of a nuclear magnetic resonance contrast agent. The composites can be used as hydrophobic drug carriers and are large in drug loading capacity; the photosensitizer molecules Ce6 for modifying the surfaces can generate singlet oxygen under excitation of a 632.8nm of laser, can effectively kill cancer cells, and can be applied to photodynamic therapy.
CN102558022A Substituted isoindoline-1,3-dione derivative The invention relates to a novel substituted isoindoline-1,3-dione derivative and the pharmaceutically acceptable salts thereof. More particularly, the invention relates to a novel substituted isoindoline-1,3-dione derivative used as an analogue of apremilast. The invention further provides a composition containing the compound disclosed by the invention and a carrier, and the application of the disclosed compound and composition in a method for beneficially treating diseases and conditions by administering apremilast.
EP1083914B1 Using ngali nut oil to treat/relieve the pain of arthritis and other similar conditions A method for treatment of the manifestations of arthritis in a mammal, including a human, by administering an effective amount of Ngali Nut Oil.
CN102690278A Novel pyrimidine-fused cyclic compounds as cytokine inhibitors The invention provides novel pyrimidine-fused cyclic compounds with low molecular weights and compositions thereof as cytokine inhibitors. In particular, the compounds summarized in the invention can be used as anti-inflammatory agents. The invention further provides a method for preparing this kind of medicaments and an application of the medicaments in preventing or treating diseases mediated by cytokines. The diseases comprise arthritis, aches, angiocardiopathy, and cancers.
CN103242341A Thieno 2,4-substituted pyrimidine compound, and pharmaceutical composition and application thereof The invention discloses a thieno 2,4-substituted pyrimidine compound of which the general formulas are (I), (II), (III) and (IV), or pharmaceutically acceptable salt or stereisomer or a prodrug molecule, and a pharmaceutical composition and application thereof. The thieno 2,4-substituted pyrimidine compound can effectively restrain abnormal expression of Aurora kinase, has specific inhibited effect on Aurora-A and Aurora-B, can be applied to a novel field of molecular targeting treatment, and has strong inhibitory activity on an excessive hyperplasia disease, especially cervical tumor cells, human macrophage line leukemia cell, and human t-lymphocyte line cancer cell.
US20090076145 Deuterium-enriched amibegron The present application describes deuterium-enriched amibegron, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20120010201 Novel anellated pyridine compounds The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.
WO2011006886A3 Azole derivatives as agricultural fungicides The present invention relates to novel azole compounds of the formulae I and Il as defined below which carry a sulfur substituent, to agricultural compositions containing them, to their use as fungicides and to intermediate compounds used in the method of producing them.
US8084477 Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with β-amyloid peptide.
US8633221 Method of enhancing lysosomal α-galactosidase A A method of enhancing the activity of lysosomal α-Galactosidase A (α-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related compounds.
WO2006028120A1 Preventive/remedy for obesity It is intended to provide a preventive/remedy for obesity, and a material for drugs and so on which can exert effects of preventing and improving the onset of various life style-related diseases such as hyperlipemia and has a high safety and a broad application range. Namely, a preventive/remedy for obesity, a visceral fat accumulation inhibitor, an agent controlling an increase in blood glucose level, an agent controlling an increase in blood insulin level, a preventive/remedy for diabetes, an agent improving fat metabolism and an agent promoting fatty acid oxidation each comprising waxy corn starch as the active ingredient.
US20110105562 Alkynyl derivatives useful as dpp-1 inhibitors The present invention is directed to novel alkynyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
CN103073501A Ornidazole crystal compound The invention provides a new ornidazole crystal (having a molecular formula of C7H10ClN3O3). The solubility of the new ornidazole crystal in water is improved to a certain degree, the stability of the new ornidazole crystal is good, and the medicine safety is improved. The invention also provides a preparation method of the new crystal, a medicinal composition containing the new crystal and a preparation containing the new crystal.
WO2009068567A1 C2-c5-alkyl-imidazole-bisphosphonates C2-C5-Alkyl-substituted [(imidazol-1 -yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula (I), wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
EP1545551A1 Delivery of modulators of glutamate-mediated neurotransmission to the inner ear The invention features methods and devices for local delivery of agents that modify glutamate-mediated neurotransmission to the inner ear for treatment of inner ear disorders caused by glutamate-induced hearing loss and/or tinnitus.
CN103254448A Medical sodium hyaluronate gel and preparation method thereof The invention provides a preparation method of medical sodium hyaluronate gel. The method comprises the following steps: a, weighing sodium hyaluronate sterile dry powder; b, under sterile processing condition, dissolving 0.7-0.9% of an osmotic pressure adjustor and 0.11-0.33% of a buffering agent based on water for injection in the water for injection, sterilizing, degerming and filtering; c, under sterile processing condition, preparing the sodium hyaluronate sterile dry powder obtained by the step a in the degermed and filtered buffer liquor in concentration of 10-40mg/ml, and sealing; d, stirring at 0-4 DEG C for 2-6 hours; and e, packaging and sterilely packing to obtain the medical sodium hyaluronate gel. The invention further provides the medical sodium hyaluronate gel prepared by the method and a medical composition containing the gel. According to the method, sodium hyaluronate is dissolved at 0-4 DEG C, particularly, sodium hyaluronate is dissolved by using an ice-bath dissolving method, and the whole dissolving time is 2-6 hours. The quality of final product satisfies the national standard of quality, and the risk in the product production process is greatly reduced, and meanwhile, the production time and energy consumption are reduced.
EP1867633A1 Polyamine analogues as therapeutic and diagnostic agents Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.
US7078040 Administering to animal or man of at least one type of xanthophyll in an amount inhibiting the expression of inflammatory cytokines and chemokines in animal or man A method of inhibiting the expression of inflammatory cytokines and chemokines in an animal or man, is disclosed. The method comprises administration to said animal or man of at least one type of xanthophyll, e.g. astaxanthin, in an amount inhibiting the expression of inflammatory cytokines and chemokines in said animal or man. Use of at least one type of xanthophyll, such as astaxanthin, for the preparation of a medicament for the prophylactic and/or therapeutic inhibition of the expression of inflammatory cytokines and chemokines in an animal or man, is described. Further, a commercial package containing a medicament comprising at least one type of xanthophyll, e.g. astaxanthin, and written and/or data carrier instructions for administration to an animal or man of the medicament for the prophylactic and/or therapeutic inhibition of the express of inflammatory cytokines and chemokines, is disclosed.
WO2012027603A3 Therapeutic consumable compositions for reduction of facial flush effect incident to alcohol consumption in persons with deficient activity of the aldehyde dehydrogenase gene-aldh2 Therapeutic consumable compositions reduce facial flush effect incident to alcohol consumption in some persons of Asian descent or persons with ALDH2 gene deficiency.
US6982270 1-Phenyl-2-oxo-3,4-dihydro-6-phenylaminoquinazoline for example; cytokine suppressive anti-inflammatory drugs; combination therapy Substituted quinazolinone compounds of formula (I) and compositions thereof for use in therapy as CSBP/p38 kinase inhibitors.
US20130065943 Compositions and methods for inhibiting expression of cd45 gene The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of the CD45 gene.
WO2006073181A1 Cell activator, cell death inhibitor and cell death promoter A cell activator or a cell death inhibitor comprising Wnt5a and/or Wnt10a as the active ingredients. A cell activator, a cell death inhibitor or a cell death promoter which indirectly acts on a target cell by controlling the secretion of Wnt5a and/or Wnt10a from the cell is also included therein. In the above-described cell activator or cell death inhibitor, orange, etc. may be used as a substance promoting the secretion of Wnt5a from a cell while echinacea may be used as a substance inhibiting the same. It is furthermore intended to provide a hair growing agent, a hair nourishment and a hair growth stimulant comprising the cell activator or the cell death inhibitor as described above as an active ingredient and a hair removal agent comprising the cell death promoter as described above as the active ingredient.
WO2014151752A1 Composition and methods for the treatment of peripheral nerve injury Provided herein are methods of treating a peripheral nerve injury in a subject. The methods include administering to the subject at or near the site of the peripheral nerve injury an effective amount of a composition comprising an agent that promotes remyelination of the peripheral nerve. Also provided are methods of determining whether a peripheral nerve injury has a capacity for recovery. The methods include selecting a subject with a peripheral nerve injury, administering to the subject a first dose of a composition comprising and agent that promote remyelination and detecting after the first dose one or more characteristics of peripheral nerve recovery, the presence of one or more characteristics of peripheral nerve recovery indicating a peripheral nerve injury has a capacity for recovery and the absence of characteristics of peripheral nerve recovery indicating a peripheral nerve injury without a capacity for recovery.
US7166606 Certain 1-(D-cycloproplyglycinyl)-4-piperidin-4-yl)piperazine compounds as inhibitors of the serine protease factor Xa The compounds of formula (I) in which R represents a hydrogen atom or a fluorine atom, or a pharmaceutically acceptable salt thereof are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
WO2013074641A1 Piperidinyl- substituted cyclic ureas as gpr119 modulators Compounds of Formula I: and pharmaceutically acceptable salts thereof, in which X1, X2, R3, R4, R5, Rx, R7, R9, R10 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
CN102309472A Compound essential oil with anti-free radical function The invention relates to compound essential oil with an anti-free radical function. The compound essential oil comprises the following components of dl-citronellol, eugenol, citral, eugenol methyl ether and thymol. A measurement method which is widely used for analyzing the anti-oxidation capacity of substances comprise the following step of: detecting the capacity of eliminating 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radicals, the capacity of eliminating 2,2'-azino-bis(3-ethylbenzthiazoline-6-suphonic acid)<+>(ABTS<+>) free radicals, the capacity of chelating metal ions and reduction capacity, so the condition that the compound essential oil really has high anti-free radical capacity and anti-oxidation capacity is proved.
WO2010139979A3 Processes for preparing crystalline forms of dasatinib The present invention relates to intermediates and their preparation, for use in the manufacture of pure dasatinib, in particularly dasatinib monohydrate and anhydrous dasatinib. The invention also relates to pharmaceutical compositions comprising pure dasatinib and their use in the treatment of cancer.
CA2143486C Method of improving the immune response The invention provides diet supplements for pre-operative treatment of patients due for surgery.
US20050192309 Method of preventing abuse of opioid dosage forms The invention relates in part to a method of reducing the abuse potential of an oral dosage form of an opioid analgesic, wherein an analgesically effective amount of an orally active opioid agonist is combined with an opioid antagonist into an oral dosage form which would require at least a two-step extraction process to be separated from the opioid agonist, the amount of opioid antagonist including being sufficient to counteract opioid effects if extracted together with the opioid agonist and administered parenterally.
CN103435554A 2-phenylaminobenzimidazole compound and application thereof The invention relates to the field of pharmaceutical chemistry, in particular to 2-phenylaminobenzimidazole compounds, a preparation method of the compounds, medicinal compounds containing the compounds and medical application of the compounds.
EP1439179B1 New oripavine derivatives and their uses as medicines The present invention disclosed oripavine derivatives of formula (I) and their nontoxic pharmaceutical acceptable salts. In the formula (I), R1 is hydrogenatom and methyl, R2 is methyl, cyclopropyl, cyclobutyl or allyl. R3 is thiophenethyl, cycloalkyl methyl wherein cycloalkyl have 3 to 6 carbon atoms. These compounds can be used in preparing analgesics or abstinence agents of opium habit-forming drugs.
WO2011052715A1 Modified double-stranded polynucleotide A double-stranded polynucleotide composed of a sense-strand polynucleotide that comprises a nucleotide sequence complementary to a target sequence contained in a target gene and an antisense-strand polynucleotide that comprises a nucleotide sequence complementary to the sense-strand polynucleotide, wherein an aryl or heteroaryl compound is bound to a phosphate group located at the 5'-terminal of the antisense-strand polynucleotide.
CN101991839A Bone-strengthening musk analgesic paste and fingerprint measuring method of semi-finished products thereof The invention relates to a method for monitoring the quality of bone-strengthening musk analgesic paste from a semi-finished product to a finished product, which discloses and builds a building method of fingerprint of the semi-finished product and the finished product of the bone-strengthening musk analgesic paste and a standard HPLC (High Performance Liquid Chromatography) fingerprint thereof. The method comprises the following steps: firstly preparing semi-finished product and finished product solutions for test of the bone-strengthening musk analgesic paste; then, establishing the semi-finished product and finished product standard fingerprint of the bone-strengthening musk analgesic paste by an HPLC method; measuring the semi-finished product fingerprint of the bone-strengthening musk analgesic paste by the HPLC method, and comparing with the standard fingerprint, wherein batches conforming to the whole similarity enter next work procedure, and batches with the whole similarity between the fingerprint and the standard fingerprint conforming to the requirements in of the finished plaster to be measured are qualified products. The method is simple, convenient and stable, can hold the quality condition of the bone-strengthening musk analgesic paste from the whole printing characteristic and can be used as the quality control index of the bone-strengthening musk analgesic paste.
US20090088436 P38 Kinase Inhibiting Agents Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
US20100266679 Crystalline modifications of n-alpha-(2,4,6-triisopropylphenylsulfonyl)-3-hydroxyamidino- (l)- phenylalanine 4-ethoxycarbonylpiperazide and/or salts thereof The present invention relates to novel crystalline modifications of N-α-(2,4,6-triisopropylphenyl-sulfonyl)-3-hydroxyamidino-(L)-phenylalanine 4-ethoxy-carbonylpiperazide and/or salts thereof, which can be used as pharmaceutical agents, and to pharmaceutical compositions and pharmaceutical uses comprising these novel crystalline modifications.
EP2430029A1 Thieno [2, 3-b]pyridine derivatives as viral replication inhibitors The present invention relates to a series of compounds of formula (A) having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.
WO2013013640A1 Quinazoline derivative, preparation method therefor, intermediate, composition and application thereof Disclosed are as represented by Formula (I) a quinazoline derivative and a pharmaceutical acceptable salt thereof, or, an enantiomer, a non-enantiomer, a tautomer, a racemate, a solvate, a metabolic precursor, or a prodrug of both. Also disclosed are a preparation method therefor, an intermediate, a pharmaceutical composition having the quinazoline derivative, and an application thereof. The quinazoline derivative of the present invention is provided with improved anti-tumor activity.
CN103690537A Novel medicinal application of piperine The invention discloses application of piperine to preparation of a medicament for treating ulceration. The piperine has a remarkable treatment effect on piperine, particularly ulcerative colitis, can relieve the symptoms of bloody diarrhea, stomachache, hemafecia, weight loss, emesis and the like at a certain degree, and can effectively repair colonic tissue injuries due to inflammation.
CN101863891A Trifluoromethane triazolidine quinoxaline derivative and preparation method thereof The invention provides a trifluoromethane triazolidine quinoxaline derivative, which is obtained through the sequential reaction of the trifluoromethane triazolidine quinoxaline with acid or alkali metal elements or ammonium (ammonia) compounds or amino acid or alkamine, or direction reaction with acid salts. When the acid or the acid salts are sulfate radicals, trifluoromethane triazolidine quinoxaline sulfate complex salts are obtained. When the acid or acid salts are phosphate radicals, trifluoromethane triazolidine quinoxaline phosphate complex salts are obtained. The method of the invention has the advantages of reasonable design, stable process and good production feasibility. The trifluoromethane triazolidine quinoxaline derivative provided by the invention has the obvious advantages of good solubility, high bioavailability and the like, and can be prepared into preparations. After the oral administration, the trifluoromethane triazolidine quinoxaline enters the blood, the absorption is fast, and the effect taking is fast, so better diabetes treatment effect can be obtained. The trifluoromethane triazolidine quinoxaline derivative of the invention has the structural general formula as the accompanying drawing.
CN103408528A Chroman compound, as well as preparation method and application thereof The invention discloses a chroman compound, as well as preparation method and application thereof. The chroman compound is R-3-ethyl-6,8-dihydroxy-7-methyl-3,4-dihydroisochromen-1-one. The preparation method of the compound comprises the steps that: ground beetles are leached in an organic solvent, such that a leachate is obtained; the leachate is extracted; the extract liquid is concentrated, such that an extract paste is obtained; and the extract paste is separated and purified, such that the chroman compound is obtained. According to the invention, the chroman compound with novel structure is separated and identified from ground beetles. The compound has wide pharmacological activities, and can be used in preparing antitumor medicines, tumor-preventing health-care foods, anti-tyrosinase medicines, whitening cosmetics, and pheromones.
EP2010525A2 Diketo-piperazine and piperidine derivatives as antiviral agents This disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof; (I) wherein: A is selected from the group consisting of: (II) having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HTV and AIDS.
CN102988391A Application of Houttuynoid E to preparation of medicine for treating osteoporosis caused by lack of antiestrogen The invention discloses a new application of Houttuynoid E to prevention and treatment of osteoporosis which is one of serious diseases damaging human health. Along with aging of population, patients suffering from the osteoporosis increase gradually, and huge social, medical and economical burden is caused to the world. Although relevant experts and scholars at home and abroad attach importance to the prevention and treatment of the osteoporosis, an effective medicine for treating the osteoporosis still does not exist. In vivo tests show that the Houttuynoid E has an obvious anti-osteoporosis effect. Experimental results show that the Houttuynoid E can restrain bone turnover rate enhancement caused by ovariectomy so as to cause less bone destruction, and can improve the concentration of blood calcium so as to facilitate bone deposition. The Houttuynoid E has a treatment effect to the osteoporosis caused by lack of antiestrogen and avoids side effects of oestrogen.
CN101537002B Diacerein composition with good leaching property, and preparation and use thereof The invention relates to a diacerein composition with good leaching property, and preparation and a use thereof. The diacerein composition consists of diacerein and pharmaceutically acceptable adjuvants. The pharmaceutically acceptable adjuvants are selected from one or more from starch, microcrystalline cellulose, lactose, a disintegrating agent, a lubricant, an edulcorant and an adhesive. The diacerein composition quickly enters a blood circulation system more easily than an imported diacerein capsule, has better storage stability and is suitable for application to preparing drugs for preventing and treating arthritis, nephritis, glomerulonephritis and psoriasis as well as an interleukin-1 inhibitor.
EP1746082A1 Salts of zinc and aliphatic haloid carboxylic acids for therapy of skin neoplasms and visible mucous coats The invention relates to medicine, and more particularly to dermatology, namely to new salts of zinc and aliphatic haloid carboxylic acids which can be used to treat benign skin lesions and visible mucous coats. The following chemical formula of salts of zinc and aliphatic haloid carboxylic acids is proposed wherein in formulae Fluorine (F), Chlorine (Cl), Bromine (Br) or Iodine (J) can be a halogen atom. The obtained technical result is the creation of a unique preparation to treat benign skin lesions and visible mucous coats. The preparation is low-toxic, fast acting with a pronounced therapeutic effect and a good tolerance. It causes no complications during therapy, and ensures healing without scar tissue formation. The created preparation allows to extend the assortment of drugs for therapy of similar diseases.
CN102690317A Derivant of 30-halogenated betulinic acid and preparation method and application thereof The invention provides a nitrogen-heterocyclic derivant of betulinol, with a formula as showed in (1), wherein in the formula, R2 is selected from H. The invention further provides a preparation method of the derivant and the application of the derivant in preparing antineoplastic drugs.
CN102178976A Youlikang The invention discloses Youlikang comprising polyvinyl butyral, benzyl alcohol, salicylic acid, vegetable oil and anhydrous alcohol. Firstly, polyvinyl butyral is added into benzyl alcohol and is stirred fully and uniformly; then the stirred materials are added into anhydrous alcohol, and are mixed and dissolved; finally, salicylic acid and vegetable oil are added into the dissolved materials in turn, and are stirred to allow uniform dispersion so as to obtain the preparation of the invention. The Youlikang of the invention is specifically used for treating viral diseases such as condyloma acuminatum, etc.
CN1879676A Compound spray for treating rhinitis and preparation method thereof Disclosed is a compound mist for treating rhinitis and its preparation method, wherein each 1000ml of the water solution contains 300g of ethanol extract of green chiretta, 100g aqueous extract of centipede, 5g d-pesudoephedrine hydrochloride, 1.5g of diphenhydramine hydrochloride, 10ml of peppermint oil, 10ml of eucalyptus oil, 30g of polyvidon K3O, 40g of polysorbate-80, 5.7g of sodium chloride and 2g of potassium sorbate.
US7037652 Diagnosing prostate cancer in humans; obtain tissue sample, monitor gene expression, compare to control, evaluate for cancer The invention relates to methods for detecting, characterizing, preventing, and treating prostate cancer. KIAA markers are provided, wherein changes in the levels of expression of one or more of the KIAA markers is correlated with the presence of prostate cancer.
US7323478 Phenylcycloalkylmethylamino and phenylalkenylamino derivatives, including 1-phenyl-2-aminomethylcyclopropanes; therapy of metabolic, feeding, and sexual disorders including obesity Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.
WO2007034210A8 Deglycosylated anti-muc-1 antibodies and uses thereof A modified antibody molecule which selectively binds to a specific target, the antibody molecule being modified at, at least one amino acid residue that forms part of a glycosylation site in the variable region of an unmodified parent antibody molecule, characterised in that the modified antibody is not glycosylated at the previous glycosylation site of which the amino acid modification forms part and the modified antibody exhibits a greater binding affinity for the specific target than the unmodified parent antibody molecule. There is also provided nucleotide sequences, amino acid sequences and expression vectors encoding the modified antibodies, and uses thereof.
CN103127524A Preparation method of polyamide-amine dendrimer-loaded alpha-Tos The invention relates to a preparation method of polyamide-amine dendrimer-loaded alpha-Tos. The method comprises the steps that: an EDC solution is added into an alpha-Tos solution; a reaction is carried out, such that a solution is obtained; a fifth-generation polyamide-amine dendrimer solution is added into the solution, and a reaction is carried out, such that G5.NH2-alpha-Tos is obtained; triethylamine and acetic anhydridethe solutions are added into the G5.NH2-alpha-Tos solution, and a reaction is carried out, such that G5.NHAc85-alpha-Tos is obtained; the G5.NHAc85-alpha-Tos solution is added into an FI solution, and a reaction is carried out, such that G5.NHAc85-alpha-Tos-FI is obtained; EDC is added into an FA solution, and the mixture is stirred; and the mixture is added into a DMSO solution of G5.NHAc85-alpha-Tos-FI, and a reaction is carried out under stirring, such that the product provided by the invention is obtained. The preparation method provided by the invention is simple, and the method is suitable for large-scale productions. The product has a targeting treatment effect against cancer cells with high folic acid receptor expression.
CN101401901A Compound formulation for medicament for dispelling wind and treating detumescence The invention relates to a method for dispensing a medicament for dispelling wind and removing swellings. 0.1 to 0.3 percent of herba schizonepetae, 0.1 to 0.3 percent of parsnip, 0.1 to 0.3 percent of angelica, 0.1 to 0.3 percent of radix rehmanniae, 0.1 to 0.3 percent of radix sophorae falvescentis, 0.1 to 0.3 percent of rhizoma atractylodis, 0.1 to 0.3 percent of cicada ecdysis, 0.1 to 0.3 percent of til kernel, 0.1 to 0.3 percent of burdock, 0.1 to 0.3 percent of rhizoma anemarrhenae, 0.1 to 0.3 percent of gypsum, 0.1 to 0.2 percent of akebia stem and 0.1 to 0.2 percent of liquorice are adopted and prepared according to mixture ratio to obtain the medicament for dispelling wind and removing swellings. The method has the remarkable efficacies on dispelling wind, clearing heat away and removing moistness and swellings.
US20110076274 Materials and methods relating to a g-protein coupled receptor The present inventors demonstrate that the G-protein coupled receptor 55 (GPR55) is highly expressed in human aggressive breast cancer cells, and that the expression level may be correlated with the invasiveness and metastatic potential of these cells (for example metastasis to bone). In various aspects of the invention there are disclosed diagnostic tools or biomarkers that relate to the metastatic profile of breast cancer tumours. The invention also relates to pharmacological agents targeting this receptor for the purposes of inhibiting progression and spread of breast cancer.
US20110189120 Aegyptin and uses thereof The present invention relates to the discovery of the Aegyptin gene and Aegyptin protein, a molecule that interacts with collagen and inhibits platelet adhesion, activation and aggregation. Novel biological tools, prophylactics, therapeutics, diagnostics, and methods of use of the foregoing are also disclosed.
WO2014009222A1 Combination therapy for the treatment of cancer and immunosuppression The invention relates to novel Rauwolfia alkaloid derivatives of formula (I) combinations of Rauwolfia alkaloid derivatives and a mitochondrial inhibitor, e.g. metformin, and the use of Rauwolfia alkaloid derivatives in combination with mitochondrial inhibitor for the treatment of cancer and for achieving clinical immunosuppression. The invention also relates to a fluorescence-based method for predicting the sensitivity of a cancer cell towards a compound of formula (I).
EP1530476A1 Use of reboxetine for the treatment of hot flashes This patent application describes a method for treating or preventing hot flashes in a patient suffering therefrom comprising administering a therapeutically effective dose of a compound selected from reboxetine, S,S-reboxetine or pharmaceutically acceptable salts thereof, to the patient.
CN101204369A Sorafenib sustained-release implant treating for solid tumor The invention relates to a Sorafenib sustained-release implant for treating a solid tumor, which is characterized in that: the sustained-release implant contains an effective anticancer amount of Sorafenib and sustained-release excipients and a certain amount of sustained-release regulators. The solid tumors comprise the esophageal canner, the gastric canner, the breast canner, the ovarian canner, the prostate canner, the bladder canner, the liver canner, the lung canner, and the rectum canner. The sustained-release excipients are mainly a copolymer of glycollic acid and hydroxyacetic acid and one of the two materials, polifeprosan and poly-(L-lactide-co-ethyl phosphonate), or a combination of the two materials, in the process of the degradation and absorption of which the Sorafenib is continuously released to part of the tumor, thus the entire toxicity of the Sorafenib is significantly reduced while an effective medicine consistency is maintained on part of the tumor. That the sustained-release implant is implanted inside part of the tumor can not only reduce the entire toxicity of the Sorafenib but also enhance the medicine consistency on part of the tumor, thereby increasing the curing effect of non-operative therapeutics such as chemotherapeutic drugs and radiotherapy.
CN103570671A Efficient blood glucose reducing compound as well as preparation and application thereof The invention discloses an efficient blood glucose reducing compound as well as a preparation and an application thereof. The structure of the compound disclosed by the invention is shown in a formula I, in the formula, R1, R2, R3 and R4 are defined in specification and claims. The invention further discloses the preparation method of the compound shown in the formula I. The compound shown in the formula I has an inhibiting activity to SGLT (Sodium-Glucose-Linked Transporter), and can be effectively used for preventing or treating diseased related to hyperglycemia.
US20110077229 Steroid Containing Drug Delivery Systems Pharmaceutical composition for intraocular use comprising a glucocorticoid derivative, such as beclomethasone 17,21-diproprionate admixed with a biodegradable polymer such as a poly(lactide-co-glycolide) polymer or a high molecular weight polymeric hyaluronic acid are disclosed.
CN102078419A Medicament for preventing and treating porcine reproductive and respiratory syndrome (PRRS) and preparation method thereof The invention discloses a medicine for preventing and treating porcine reproductive and respiratory syndrome (PRRS). The medicament is prepared by smashing and uniformly mixing the following main crude drugs in parts by weight: 9-11 parts of pine needles, 1.5-2.5 parts of dried tangerine or orange peel, 0.8-1.2 parts of white ginseng, 0.8-1.2 parts of scutellaria baicalensis, 0.8-1.2 parts of golden cypress, 1.5-2.5 parts of gardenia jasminoides ellis, 1.5-2.5 parts of isatis root, 0.2-0.4 part of liquorice, 1.5-2.5 parts of honeysuckle flower, 1.5-2.5 parts of oriental wormwood, 3.5-4.5 parts of milkvetch root, 1.5-2.5 parts of cyrtomium rhizome, 0.8-1.2 parts of fructus forsythiae, 1.5-2.5 parts of platycodon grandiflorum, 0.8-1.2 parts of giant knotweed rhizome and 0.3-0.5 part of milkvetch root polysaccharide. The medicament has a better preventing function on pigs which are not infected by the PRRS, has a good therapeutical effect on pigs which suffer from moderate PRRS and also has an obvious control effect on swine influenza, swine streptococcosis and swine erysipelas.
US20120065209 TETRAHYDRO-IMIDAZO[1,5-a]PYRAZINE DERIVATIVES SALTS, PREPARATION METHODS AND MEDICINAL USE THEREOF Pharmaceutically acceptable salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed.
US6936609 Hydrolase enzyme inhibitors comprising nitrogen compounds such as 2-(3,4-Dimethoxyphenyl)-7-(1-ethylpropyl)-5-methyl-4-(3,4,5-trimethoxyphenoxy)-imidazo[5,1-f][1,2,4]triazine, used for prophylaxis of neurodegenerative disorders The invention relates to new imidazotriazines, processes for their preparation, and their use for the production of medicaments for the treatment and/or prophylaxis of neurodegenerative disorders, in particular Parkinson's disease.
EP2475392A1 Methods for treating irritable bowel syndrome (ibs) The present invention provides new methods and kits for treating IBS; treating IBS in females; treating IBS in older subjects; and treating IBS in non-white subjects.
US20080242628 In vivo The present invention relates to the specific inhibition of gene expression in mammals by bringing the target gene into contact with double stranded RNA (dsRNA).
US20120095022 Derivatives of 10-amino-1,2,3,4-tetrahydropyrido[2,1-a]isoindol-6(10bh)-ones, method for preparation thereof and therapeutic uses thereof The present invention relates to compounds having the following general formula (I): wherein: A represents a SO2 or CX group, X representing O or S; R1, R2, R″, R4 represent in particular H, R represents in particular an alkyl group or an aryl group, as well as to the pharmaceutically acceptable salts thereof, the compound of formula (I) taking the form of a pure stereoisomer or an enantiomer and/or diastereoisomer mixture, including racemic mixtures.
WO2010122071A1 Thia-triaza-cyclopentazulenes as pi3-kinases inhibitors for the treatment of cancer The present invention encompasses compounds of general formula (1) wherein 5 R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
US20090036518 Pharmaceutical composition containing flavonoids A pharmaceutical composition is provided, where the pharmaceutical composition contains formula (I), (II), or (III) flavonoids which possess (PDE4), as a main ingredient. Especially, this composition has a binding affinity of high affinity rolipram binding sites (HARBS) of a PDE4 lower than a binding affinity of low affinity rolipram binding sites (LARBS) of the PDE4 is used in the treatment of asthma, chronic obstructive pulmonary disease (COPD), or chronic inflammation, and has bronchodilatory effects. In addition, whether the above-mentioned flavonoids have side effects, such as nausea, vomiting, gastric hypersecretion, etc., in accordance with their binding affinity to HARBS of particulates of brain cells are disclosed.
CN102048710A Quickly dissolved film and preparation method thereof The invention relates to a quickly dissolved film. The film is characterized by consisting of 0.01 to 90 percent of frovatripan serving as an active ingredient and the balance of film forming material and medicinal auxiliary materials. A preparation method comprises the following steps of: dissolving frovatripan and polymer in water or organic solvent or suspending other auxiliary materials, coating the solution on silicon rubber paper or a proper carrier, and drying for 0.5 to 4 hours at the temperature of between 35 and 65 DEG C; and performing shearing or film pressure separation on the dried semi-finished product to obtain the film of the specified size.
US20080255085 Novel Imidazo [4,5-b] Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase 3 for Use in the Treatment of Dementia and Neurodegenerative Disorders Compounds of formula I wherein X is or Y; and wherein A, Y, R1, R2, R3, R4 and R5 are as defined in the specification as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
CN103230471A Externally used drug for treating burns and scalds and preparation method thereof The invention discloses an externally used drug for treating burns and scalds. The drug is prepared from the following raw materials in parts by weight: 10-20 parts of cornu bubali powder, 10-20 parts of radix rehmanniae, 20-30 parts of radix arnebiae, 5-8 parts of borneol, 20-30 parts of calcined gypsum, 10-20 parts of Sichuan lovage rhizome, 30-40 parts of rhubarb root and rhizome, 5-10 parts of safflower and 20-30 parts of red paeony root. A preparation method of the drug comprises the steps of (a) grinding the raw materials into powder respectively; (b) adding the cornu bubali powder, radix rehmanniae, radix arnebiae, Sichuan lovage rhizome, rhubarb root and rhizome, safflower and red paeony root in the step (a) to sesame oil, stirring the mixture, and heating the mixture to 80-100 DEG C to obtain first drug oil; (c) cooling the first drug oil obtained in the step (b) to 40-60 DEG C, adding beewax, and stirring the mixture to obtain second drug oil; and (d) cooling the second drug oil to 18-22 DEG C, adding the borneol and calcined gypsum in the step (a), and stirring the mixture uniformly, thus obtaining the externally used drug for treating burns and scalds. The externally used drug provided by the invention has good treatment effects, avoids scars after cure, and is suitable for I, II and III-degree burns and scalds.
WO2009060452A2 Methods and compositions for treating biliary cholesterol crystallization and related conditions The present invention is directed to the field of treating conditions related to biliary cholesterol crystallization, particularly to the administration of inhibitors of Stearoyl Coenzyme A Desaturase 1, wherein the inhibitor of SCD1 enzymatic activity is not a fatty acid bile acid conjugate (FABAC).
WO2013080046A1 Lurasidone novel dosage regimens and use thereof for the treatment, prevention, and/or management of at least one cns disorder Dosage regimens for at least one compound chosen from Iurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof are disclosed as are kits and methods for treatment and/or prevention of at least one CNS disorder such as, for example, mixed depression and bipolar disorder, and management of at least one CNS disorder, such as improving quality of life and reversing impairment in learning and memory associated with schizophrenia, comprising administering to a patient a therapeutically or prophylacticaily effective amount of at least one compound chosen from lurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof.
US7012085 As antipsychotics in therapy of schizophrenia, depression, bipolar disorders, cognition deficits, Parkinson disease, drug abuse, attention deficit hyperactivity disorders, glaucoma, diabetes and erectile dysfunction The invention provides compounds of formula (I) wherein R0, R1, R2 and A are as defined in the description, and the preparation thereof. The compounds of formula (I) have high affinity as α2 adrenoceptors and hence are useful as pharmaceuticals.
US20100112014 Novel hydrogel compositions and methods of using Disclosed are novel agarose, methylcellulose, and dextran hydrogels. Further disclosed are methods of making and using the hydrogels.
US20120029055 Modulators of apoptosis and the uses thereof Here we demonstrate that miR-125b, a brain-enriched microRNA, is a negative regulator of p53 in animals. miR-125b-mediated downregulation of p53 is dependent on the binding of miR-125b to a microRNA response element in the 39 untranslated region of p53 mRNA. Overexpression of miR-125b represses the endogenous level of p53 protein and suppresses apoptosis in cells. In contrast, knockdown of miR-125b elevates the level of p53 protein and induces apoptosis in cells. This phenotype can be rescued significantly by either an ablation of endogenous p53 function or ectopic expression of miR-125b in zebrafish. Ectopic expression of miR-125b suppresses the increase of p53 and stress-induced apoptosis. Together, our study demonstrates that miR-125b is an important negative regulator of p53 and p53-induced apoptosis during development and during the stress response.
US20110053982 Ether benzylidene piperidine 5-membered aryl carboxamide compounds useful as faah inhibitors The present invention relates to compounds of the Formula (I), and pharmaceutically acceptable salts thereof, and their use in the treatment of FAAH-mediated diseases or condition.
WO2004105763A3 Use of tyrosine kinase inhibitor to treat diabetes The invention relates to the use of a c-Abl-. PDGF-R-, or c-kit- tyrosine kinase inhibitor, e.g. 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, Bis (1H-2-indolyl)-1-methanones, AG1295, CT52923, RP-1776; GFB-111; pyrrolo[3,4-c]-beta-carboline-diones, SU 102, AG1296, RPR101511A, CDP 860, Zvegf3, CP673451, PD 170262, KI 6783, KN 1022, AG 13736, CHIR 258, MLN 518, SU 11248, Leflunomide, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of diabetes, e.g. type I diabetes, type II diabetes.
EP1714650A1 Arginine-containing compositions for increasing blood flow The object of the present invention is to provide a composition for increasing blood flow wherein side effects such as reduction of blood pressure are reduced and the blood flow can be effectively increased in the capillaries. The present invention discloses a composition for increasing blood flow containing arginine, which contains arginine in an amount ranging from 25mg/kg body weight to 150mg/kg body weight per a dose. The present invention also provides a food or a feeding stuff containing the composition for increasing blood flow.
US20120035161 Novel Compositions and Methods of Treating Diseases Using the Same The invention includes compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, treating diseases associated with activated lymphocytes, or treating PAH.
US20120059064 Compositions and Methods For Inhibiting an Isoform of Human Manganese Superoxide Dismutase The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as neurodegenerative diseases and heart failure.
EP1653957A1 Piperidine compounds useful as malonyl-coa decarboxylase inhibitors The present invention provides methods for the use of compounds as depicted by structure (I), pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCID inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.
US20120269768 Antiviral product The present invention relates to a novel antiviral product, its use in the treatment of hepatitis C, and its process of manufacture. More particularly it relates to a characterised product exhibiting antiviral activity against Hepatitis C virus (HCV). In one embodiment there is provided a single herb Astragalus extract, or an active fraction thereof, for use as an antiviral in the treatment of hepatitis C.
EP1770065A1 Sodium hydrogencarbonate crystal grains with low level of integrity and process for producing the same Sodium hydrogencarbonate crystal particles, which comprise sodium hydrogencarbonate crystal particles having an average particle size of from 50 to 500 µm based on the mass, and anhydrous sodium carbonate, and sodium carbonate monohydrate and/or Wegscheider's salt, present on the surface of the sodium hydrogencarbonate crystal particles in such amounts that the total content of anhydrous sodium carbonate, sodium carbonate monohydrate, Wegscheider's salt and sodium sesquicarbonate in the sodium hydrogencarbonate crystal particles is from 0.04 to 1 mass% as calculated as anhydrous sodium carbonate, anhydrous sodium carbonate accounts for at least 40 mass% of the total content, and sodium carbonate monohydrate and/or Wegscheider's salt accounts for from 5 to 60 mass% of the total content. Sodium hydrogencarbonate crystal particles having a low caking property, which are useful in the field of food products, pharmaceuticals, bath additives, etc., which require no necessity to contain an anticaking agent, a process for producing them and a method for packaging them, can be provided.
US20100310564 Method for the Treatment of Glomerulonephritis The present invention provides a method for the treatment and/or prophylaxis of glomerulonephritis associated with one or more disorders selected from the group consisting of Goodpasture's syndrome, a vasculitic disorder, Wegener's disease, IgA nephropathy and an inflammatory disease with basement membrane involvement comprising administering a therapeutically effective amount of agent which interacts with or modulates the expression or activity of a mammalian IL-6 polypeptide.
CN103340867A Osthole-mixing ointment, preparation method and applications The invention provides an osthole-mixing ointment, and the active components in the formula comprise osthole and ligustrazine. The ointment has a stronger inhibition effect on skin allergy, overcomes the problem of patient skin allergy directly existed in some other antiphlogistic analgesic medicines, and has a good application prospect in anti-inflammation, analgesia and eczema treatment.
US20100227832 Modulation of telomere length in telomerase positive cells and cancer therapy Induction of telomere shortening, G2 arrest and apoptosis in telomerase positive cancer cells using acyclic nucleoside analogs has been disclosed. In addition, methods for impairment or prevention of tumorigenic telomerase positive cells from having a chance to grow into a tumor and methods for promoting tumor regression (decrease in size of an established tumor) using acyclic nucleoside analogs has been disclosed.
US7273744 Heparanase-like polypeptides The present invention provides a homologue to heparanase which is present in three splice variants.
WO2008057856A2 Modulators of glucocorticoid receptor, ap-1 and/or nf-kappab activity and use thereof Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-ϰB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
WO2007129221A8 Compositions comprising an epi-inositol compounds and methods for treatment of disorders of protein aggregation The invention relates to compositions, methods and uses comprising an epi-inositol compound that provides beneficial effects in the treatment of a disorder and/or disease including a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence. In aspects of the invention, the epi-inositol compounds provide beneficial effects in the treatment of Alzheimer's disease, dementia, and mild cognitive impairment.
CN103083649A Chewing gum for preventing and treating oral ulcer resulted from chemotherapy The invention relates to a chewing gum for preventing and treating oral ulcer resulted from chemotherapy and a preparation method of the chewing gum. The chewing gum comprises chewing gum ingredients and medicaments for preventing and treating oral ulcer; every 100 grams of chewing gum for preventing and treating oral ulcer comprise the following medicaments for preventing and treating oral ulcer by weight: 5mg-10mg of recombinant human granulocyte colony-stimulating factors, 5mg-10mg of folic acid, 5mg-10mg of metronidazole, 20mg-50mg of lidocaine, 5mg-20mg of cimetidine, 2.5mg-10mg of vitamin B2, and the balance being chewing gum ingredients. The chewing gum ingredients comprise the following components in percentage by weight: 25%-30% of edible gum base, 20%-25% of malt syrup, 35%-45% of xylitol and 10%-20% of sorbitol. The chewing gum disclosed by the invention can be used for effectively preventing and treating oral ulcer resulted from different disease causes after chemotherapy, further can be used for reducing stimulus of medicaments to gastrointestinal tract, reducing adverse reactions and increasing safety. Moreover, the chewing gum is good in mouth-feel and convenient to take.
CN103588766A 1,3,4-oxadiazole-containing 3-(1H-3-indolyl)-1H-pyrazole derivatives and their preparation method and use The invention relates to 1,3,4-oxadiazole-containing 3-(1H-3-indolyl)-1H-pyrazole derivatives and their preparation method and use. The invention provides the 1,3,4-oxadiazole-containing 3-(1H-3-indolyl)-1H-pyrazole derivatives shown in the general formula Ia or Ib and their pharmaceutically acceptable salts, and also provides the preparation method of the 1,3,4-oxadiazole-containing 3-(1H-3-indolyl)-1H-pyrazole derivatives shown in the general formula Ia or Ib and a use of a composition of the one or more 1,3,4-oxadiazole-containing 3-(1H-3-indolyl)-1H-pyrazole derivatives in preparation of drugs for treating human or animal cancers.
CN103520131A Preparation method of paroxetine hydrochloride semihydrate capsule The invention provides a preparation method of a paroxetine hydrochloride semihydrate capsule. The method comprises the step of directly filling the capsule after mixing paroxetine hydrochloride with special grain size and an auxiliary material. The paroxetine hydrochloride semihydrate capsule prepared by the method provided by the invention is stable and controllable in quality, and the content uniformity satisfies the demand.
WO2013043255A1 Methods and compositions for the treatment of ovarian cancer Embodiments of the present disclosure relate to methods and compositions for treating a subject with ovarian cancer. Some embodiments include treating a subject with a particular combination of chemotherapeutic agents.
US20120282332 Composition and method thereof The present disclosure relates to a composition comprising Trigoneoside Ib and Vicenin-1 for treatment and management of Goodpasture's disease, Glomerulonephritis, Rheumatoid Arthritis, Systemic Lupus Erythematosus and Idiopathic Thrombocytopenia Purpura. The present disclosure also relates to a method of obtaining the said composition from Trigonella foenum-graecum.
EP1383494A4 Compositions and methods for the prevention and treatment of human prostate cancer The invention provides a composition and method for the prevention or treatment of mammalian prostate carcinoma using Vitamin E or Vitamin E derivatives or Vitamin E analogs and selenium or selenium salt or selenium derivative in a combined or an uncombined form, alone or in combination with traditional therapies. The invention also provides a composition and method for the prevention or treatment of mammalian prostate carcinoma using Vitamin E or Vitamin E derivatives or Vitamin E analogs and selenium or selenium salt or selenium derivatives in a combined or an uncombined form, alone or in combination with traditional therapies to increase the levels of intracellular p21 and/or p27.
US20060222689 vitamin C, vitamin B complex, carotene, vitamin E, a fragrance, a thickener and a surfactant; acne treamtent A composition for local application includes: vitamin C in an amount from about 1% to 45% w/w; vitamin B complex in an amount from about 1% to 5% w/w; carotene in an amount from about 0.1% to 3% w/w; and vitamin E in an amount from about 2% to 90% w/w. The composition may further includes 0.1-2% fragrance, 1-5% w/w thickener, 1-8% w/w surfactant.
US20100166848 Liposomal formulations for treating cancer The invention provides a pharmaceutical composition comprising liposomes which coencapsulate 5-fluorouracil (5-FU) and 2′-deoxyinosine (d-Ino). In a preferred embodiment, the liposomes comprise phosphatidylcholine (PC), phosphatidyl-glycol (PG) and sterol, preferably in a molar ratio PC/PG/sterol of 20-80/10-60/15-60. The invention further provides a method for preparing liposomes which coencapsulate 5-fluorouracil (5-FU) and 2′-deoxyinosine (d-Ino), and the use thereof for the manufacture of a medicament for treating cancer in a patient.
US20110301232 Process of extracting procyanidins by alkaline hydrolysis A process of extracting procyanidins by alkaline hydrolysis. In particular, a procyanidin-containing material, pomace or residue is treated with an alkali, such as sodium or potassium hydroxide, for a predetermined amount of time and at a predetermined temperature to release procyanidins bound to polysaccharides and/or proteins of the cell wall or depolymerize polymeric procyanidins. After the procyanidins are released by alkaline hydrolysis, the extracts are acidified to obtain a pH level where the procyanidins do not degrade. The process of extracting procyanidins may be utilized to estimate the total amount of bound procyanidins in a plant material, enhance the bioavailability of beneficial procyanidins monomers and/or to treat the residue remaining after conventional solvent extraction for increased procyanidin extraction.
US20090048190 Antiviral activity and resolution of 2-hydroxymethyl-5(5-fluorocytosin-1-yl)-1,3-oxathiolane A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.
WO2005063264A1 Immunopotentiator and method of enhancing immunological activity with the same An immunopotentiator for enhancing the immunological activity of mammals, characterized by containing as an active ingredient a nucleic acid containing a special nucleic acid base, a derivative of the acid, or a plasmid having a nucleic acid containing a special nucleic acid base.
CN102949334A Levofloxacin hydrochloride gel-type eye-drops The invention discloses levofloxacin hydrochloride gel-type eye-drops comprising levofloxacin hydrochloride, poloxamer, another auxiliary material, and water. The water is injection water. The other auxiliary material is a pH regulating agent which is one or a complex of the components selected from sodium dihydrogen phosphate, potassium dihydrogen phosphate, borax, acetic acid, sodium acetate, and sodium hydroxide. The levofloxacin hydrochloride gel-type eye-drops have high medicine concentration in cornea and aqueous humor. Therefore, the levofloxacin hydrochloride gel-type eye-drops are beneficial for controlling bacteria reproduction and growth, shortening disease course, and improving curative rate.
CN101933895A Fenticonazole nitrate vaginal suppository composition The invention discloses a fenticonazole nitrate vaginal suppository composition. By utilizing the high-efficiency antibacterial activity of the fenticonazole nitrate and adopting local vaginal administration, the antibacterial activity is greatly improved, and the toxic or side effect due to oral administration is remarkably reduced. The fenticonazole nitrate vaginal suppository composition is used for locally treating double infection caused by vulvovaginal candidiasis and gram positive bacteria. The invention also relates to a fenticonazole nitrate vaginal suppository composition and a preparation method thereof.
EP1469886B1 Lyophilized pharmaceutical composition of propofol This invention relates to a pharmaceutical compositio n containing an inclusion complex of propofol and a water soluble cyclodextrin, in freeze dried form. The invention also relates to a process for producing the composition and the composition in unit dose form.
WO2008068265A1 Novel substituted diaza spiro pyridinone derivatives for use in mch-1 mediated diseases The present invention concerns aryl and heteroaryl substituted diaza-spiro-pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.
WO2008077247A1 Coatings for implantable medical devices comprising cholesterol Disclosed herein are solid film coatings for implantable medical devices comprising a solid film covering at least a portion of the device. The solid film comprises: at least one lipid selected from cholesterol and cholesterol derivatives, at least one additional solid lipid other than cholesterol and cholesterol derivatives, and a therapeutically effective amount of at least one pharmaceutically active agent. Also disclosed herein are methods of preparing film coatings and methods of treating diseases with the implantable devices.
CN101797266B Pharmaceutical composition containing quercetin and usage thereof The invention provides the application of quercetin in the preparation of medicine for preventing or treating diseases caused by influenze virus, adenovirus, staphylococcus aureus and/or streptococcus hemolyticus and the like, and a pharmaceutical composition thereof. The pharmaceutical composition has the activity for resisting the influenze virus being equivalent to oseltamivir.
CN1938325A Synthetic membrane anchors The invention relates to synthetic molecules that spontaneously and stably incorporate into lipid by-layers, including cell membranes. Particularly, although not exclusively, the invention relates to the use of these molecule s as synthetic membrane anchors or synthetic molecule constructs to effect qualitative and quantitative changes in the expression of cell surface antigens.
CN102161648A Preparation method and applications of isoflavone type compounds with selective estrogen receptor modulating activity The invention relates to the pharmaceutical chemistry field, in particular to isoflavone type compounds (I), a preparation method of the compounds, medicinal composites with the compounds and medicinal applications of the compounds and the medicinal composites, in particular to the applications used as a selective estrogen receptor modulator.
US7067681 Nitration of tetracyclines and derivatives, then reducing, diazotizing and alkylation on the presence of palladium chloride; catalysis; antibiotics The present invention relates to novel chemistries which allow for heretofore unobtainable substituted tetracycline compounds which exhibit significant antibacterial activity. The methods disclosed herein utilize reactive tetracycline-based precursor compounds, reactive organic substituent precursors and transition metal catalysts under conditions such that a tetracycline compound substituted with the desired organic substituent is formed. In one embodiment of the invention, a substituted tetracycline compound may be prepared by combining a reactive tetracycline-based precursor compound such as an arene tetracycline diazonium salt, and a reactive organic substituent precursor, e.g., alkenes, substituted alkenes, vinyl monomers, aromatics and heteroaromatics, in the presence of a transition metal catalyst, such as palladium chloride, under conditions such that a tetracycline compound substituted with the organic substituent is formed. Such compounds may optionally act as intermediates for making other compounds, e.g., hydrogenation of unsaturated groups on the substituent.
CN101518564A Application of the effective part of astragalus hoangtchy in preparation of anti-inflammatory The invention discloses an application of the effective part of astragalus hoangtchy in preparation of anti-inflammatory, which pertains to the field of medicine. The application has the advantages of disclosing the anti-inflammatory function of the effective part of astragalus hoangtchy, especially of astragaloside IV, from a brand new point of view and mechanism thereof, being capable of developing novel anti-inflammatory on the basis and having guidance significance for clinical treatment and basic research.
US7259168 2-Aminoalkyl-thieno[2,3-d]pyrimidines The present invention relates to 2-aminomethylthieno[2,3-d]pyrimidines of the general formula (I) in which the radicals R1 to R6 have the meaning indicated in the text. The compounds show phosphodiesterase V inhibition and can be employed for the treatment of conditions of the cardiovascular system and for the treatment of potency disorders.
WO2012055995A1 Tricyclic compounds as mpges-1 inhibitors The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
WO2006052150A1 Mussel extract composition with enhanced anti-inflammatory activity This invention provides a composition containing a mussel extract and choline or a choline derivative. The composition has enhanced anti-inflammatory activity compared to the mussel extract containing no choline or choline derivative. The composition may be used for treating inflammation, particularly inflammation caused by arthritis.
US20090023628 Cosmetic Composition and a Process for Preparing This Cosmetic Composition and a Cosmetic Product The present invention relates to a cosmetic composition comprising: a wetting system that comprises at least glycerin in an amount ranging from 8.0% to 10% by weight, based on the total weight of the composition; an emollient system that comprises at least cetyl lactate and Shea butter; an emulsifying system that comprises at least steareth-2 and steareth-21; an oiliness adsorbing system that comprises at least nylon 12; and a silicone system that comprises at least cyclomethicone and cyclomethicone and dimethicone crosspolymer. This multifunctional cosmetic composition exhibits rapid absorption, properties of differentiated softness, smoothness and intensive and prolonged hydration when applied to the skin. Further, the present invention relates to a process of preparing the referred-to cosmetic composition and to a cosmetic product that comprises said composition.
CN103751144A Ornidazole vaginal effervescent tablet The invention provides an ornidazole vaginal effervescent tablet, including ornidazole, a filler, a foaming agent and a foam stabilizer, and the ornidazole accounts for 20-60 wt% in the vaginal effervescent tablet. The foaming agent comprises an acid system comprising acid or acid salt, and an alkali system comprising carbonates. The acid system includes citric acid, tartaric acid, succinic acid, fumaric acid, adipic acid, malic acid, water-soluble amino acid, potassium bitartrate, sodium hydrogen tartrate, sodium bitartrate, potassium dihydrogen?citrate, sodium fumarate and boric acid. The alkali system includes sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate, calcium bicarbonate and calcium carbonate. The foam stabilizer is a surfactant selected from sodium dodecyl sulfate and Tween 80. The ornidazole vaginal effervescent tablet provided by the invention can be used for preparation of drugs for treating vaginal infection diseases caused by sensitive anacerobes.
WO2010064422A1 Method for killing tumor by photosensitization treatment under conditions where histone is highly acetylated Disclosed is a therapeutic agent for cancer, which comprises a histone deacetylase inhibitor as an active ingredient and is intended to be used in combination with a PUVA therapy. Also disclosed is a therapeutic agent for cancer, which comprises a combination of a histone deacetylase inhibitor and a photosensitizing agent and is intended to be used in combination with a PUVA therapy. Preferred examples of the histone deacetylase inhibitor include sodium butyrate, trichostatin A (TSA), suberoylanilide hydroxamic acid (Zolinza/Volinostat/SAHA), valproic acid, Belinostat/PXD101, ITF2357, CRA-24781/PCI24781, Romidepsin/FK228/Depsipeptide, Phenylbutyrate/VP-101/EL-532, Pivanex/AN-9, SB939, MS-275/SNDX-275/entinostat, MGCD-0103 and JHJ-26481585.
US20090124832 Oligoamine compounds and derivatives thereof for cancer therapy Oligoamine compounds with anti-cancer and anti-proliferative activity are provided, as well as methods for making and using the compounds. The compounds are shown to be active against prostate cancer cell lines and against prostate cancer tumors in mice. The compounds are also useful in treatment of breast cancer and other cancers.
EP1242066B1 Use of 1-aminoindan derivatives for treatment of mania in bipolar mood disorder The subject invention provides a method of treating mania in bipolar disorder in a subject comprising administering to the subject a therapeutically effective amount of derivatives of 1-aminoindan or their racemic mixtures, enantiomers, or salts, of general formula (I).
CN1830439A Preparation method of metronidazole freeze dried powder injection A freeze-dried powder injection of metronidazole for treating anaerobe infection, Trichomonas vaginalis and amebiasis is prepared from metronidazole through depositing in water, cold storage, ultrafiltration, further preparing in dark condition and N2 atmosphere, pouring in containers, freeze drying and sealing.
WO2011110183A1 Azaisoquinolinone derivatives as nk3 antagonists The invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.
US20080234294 Administering compounds such as 1,3-Dicyclohexyl-2-(5,6-dihydro-imidazo[2,1-b]thiazol-3-ylmethyl)-isothiourea for therapy of Warts Hypogammaglobulinemia Immunideficiency Myelokathexis; neutropenia, hypogammaglobulinemia or HPV infection This invention relates to the use of a CXCR binding molecules as described in the specification, in WHIM syndrome.
US6872731 Imidazo-pyridine derivatives as ligands for GABA receptors A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH-linkage, are selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
CN103764132A Oral formulations of mitochondrially-targeted antioxidants and their preparation and use Provided are stable liquid and solid formulations of oxidized and reduced mitochondria-targeted antioxidants, and methods of their preparation and use.
CN101161654A Antineoplastic active canthardin derivative and method for preparing same The present invention discloses a novel cantharidin derivative with selective suppressive activity on tumor cells but low toxicity on human body. The present invention also discloses the preparation method of the cantharidin derivative, in which norcantharidin, glycin, and amantadine are adopted as the raw materials to synthesize the cantharidin through steps, and the preparation method is safe, simple and easily accomplishable. The cantharidin derivative with suppressive activity on tumor cells has smart structure and strong suppressive activity on tumor cells, fills in the gap in the field, makes the solid foundation for the preparation of cantharidin derivative which has selective suppressive activity on tumor cells and minor toxicity on human body, and has both potential significance on the industrialized exploit and great contribution to the research on human anti-tumor drugs.
US8715668 Antibody selective for a tumor necrosis factor-related apoptosis-inducing ligand receptor DR5 and uses thereof An antibody of the invention interacts with human DR5 to produce agonistic or antagonistic effects downstream of the receptor including inhibition of cell proliferation and apoptosis. Nucleic acid sequences and amino acid sequences of anti-DR5 antibodies have been elucidated and vectors and cells containing and expressing these sequences have been generated. Methods and uses for the antibodies are detailed including treatment of apoptosis-related disease and treatment of dysregulated cell growth.
WO2010102673A1 Hellebrin and hellebrigenin derivatives The present invention relates to new cardiotonic Steroid Compounds of Formula (I) or (II) wherein X1, X2, X3, L, R1, R2, R3, R4, and R5 have the same meaning as that defined in the Claims. The invention also relates to the use of said Compounds as medicaments, in particular in the treatment of Cancer.
WO2011133227A3 Synthetic oligosaccharides for staphyloccocus vaccine The present invention synthetic oligo-β-(1→6)-glucosamine structures and a methodology which essentially allows for the synthesis of any oligo-β-(1→6)- glucosamine species having a definite number of monosaccharide units, including a set pattern of acetylated and non-acetylated residues. The invention further provides antibodies to these synthetic oligo-β-(1→6)-glucosamines as well as compositions thereof and methods for treating and preventing infections caused by bacteria expressing poly-β-(1→6)-glucosamines, such as Staphylococcus aureus.
US20080124306 Vigor Enhancement Via Administration of Pyrimidine Derivatives Disclosed herein are methods for increasing the overall vigor of a subject, and/or vigor of target tissues of a subject. Exemplified herein is the utilization of pyrimidine derivatives which act to stimulate stem cell proliferation. In addition to increasing vigor, such stem cell proliferation agents (SCPA) may be used to enhance and/or improve the outcome of other therapies, and may be used in psychiatric applications. Increasing vigor in subjects is not necessarily targeted to the treatment of a disease, thus, the methods can include administration to clinically healthy animals.
US20130039981 Quick Dissolving, Long Acting Zinc Therapeutic Formulations The present invention comprises a quick dissolving, long acting zinc therapeutic cold formulation containing high levels of an active compound encapsulated within bioadhesive/muco-adhesive polymers as a controlled release oral drug delivery system. The composition allows for increased residence time for enhanced prophylactic and therapeutic efficacy within the mouth and oral cavity. This allows for a reduction in the number of doses necessary to achieve therapeutic relief which will result in increased patience compliance.
CN1857468A Prepn and application of haw heaf total phenolic acid composition The present invention relates to compound preparation with haw leaf flavonid composition as main component for treating cardiac and cerebral vascular diseases. The haw leaf flavonid composition contains total haw leaf phenolic acid in 1-99 wt% and gingko leaf flavonid, sowthistle-leaf ixeris flavonid, pueraria flavonid, safflower flavonid, astragalus flavonid and total saponin, total paeoniflorin or seabuckthorn flavonid in 1-99 wt%, and is compounded with pharmaceutically acceptable supplementary material to prepare pharmaceutically acceptable preparations. The medicine of the present invention is used in preventing and treating cardiac and cerebral vascular diseases, senile dementia, and other diseases.
WO2011159302A1 Arylindenopyrimidines for treating neurodegenerative and movement disorders while minimizing cardiac toxicity This invention provides novel arylindenopyrimidines of the Formula (I), and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing adenosine A1 and/or A2a receptors. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
CN103347497A Food supplement and injectable material for prophylaxis and therapy of osteoporosis and other bone diseases The invention relates to the application of inorganic polyphosphates (polyP) and complexes of polyP and calcium [polyP (Ca2+ complex)] for prophylaxis and treatment of osteoporosis and other bone diseases by inducing hydroxyapatite formation and decreasing osteoclastogenesis. PolyP and polyP (Ca2+ complex) can be used both as a drug or food supplement and as a material to be injected into bone tissue.
US7323168 Immunotherapy for chronic myelocytic leukemia Immunotherapy utilizing naked anti-granulocyte antibodies provides an effective means for treating chronic myelocytic leukemia (CML). Such antibodies can be administered alone or in combination with other therapies, such as immunoconjugates or chemotherapeutics. In either format, an effective therapy for treating CML is provided, which avoids the toxic side-effects typically associated with cancer therapy. The disclosed immunotherapy also is effective for treating acute myelocytic leukemia (AML) when co-administered with inducing agents which induce expression of antigens minimally displayed on the surface of myeloblasts.
US20120148510 Compositions and Methods for Improving the Appearance of Facial Pores A method of improving the appearance of facial pores is provided. The method includes the step of applying a composition having an effective amount of a material that regulates IL-1 and/or hyaluronic acid synthesis to an area of facial pores, wherein the composition is applied for a period of time sufficient for the material to improve the appearance of the facial pores. In some embodiments, the material that regulates IL-1 and/or hyaluronic acid synthesis is hexyldecanol. The method may also include the step of identifying facial pores on a facial skin surface.
CA2253187C Use of tempol in the prevention of photoaging A method of preventing photoaging and other types of sun damage by topically applying a composition containing Tempol is provided. Pharmaceutical compositions comprising Tempol for the prevention of photoaging and other types of sun damage are also provided.
US20110082157 Piperidinylamino-Thieno [2,3-D] Pyrimidine Compounds The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno [2,3-d] pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as pulmonary arterial hypertension, migraine, hypertension, disorders of the gastrointestinal tract, restenosis, asthma, obstructive airway disease, prostatic hyperplasia and priapism, anxiety, depression, schizophrenia, neural injury and stroke. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also provided.
CN102512664A Nerve growth factor composition The invention discloses a nerve growth factor (NGF) composition, mainly composed of NGF and alpha-linolenic acid. The preparation prepared by the composition disclosed by the invention contains 5 mug to 400 mug of NGF and 0.5 g to 300 mg of alpha-linolenic acid per unit; and a medicine for further enhancing the curative effect of the NGF is provided. Simultaneously, the composition is transferred to the nervous system by combining with a microemulsion system, and the alpha-linolenic acid and a microemulsion transfersome exert a synergistic effect, so that the efficiency of the entrance of the NGF in the blood brain barrier is greatly increased.
US20130005728 Substituted pyrimidines as prostaglandin d2 receptor antagonists The present invention is directed to a substituted pyrimidine compound of formula (I) or an enantiomer thereof, or a prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound.
EP1461040B1 Succinic acid salts of 5,8,14-triazatetracyclo[10.3.1.0 2,11 .0 4,9 ]-hexadeca-2(11),3,5,7,9,-pentaene and pharmaceutical compositions thereof The present invention is directed to the succinate salts of 5,7,13-triazatetracyclo[9.3.1.02,10.04,8]-pentadeca-2(10),3,5,8-tetraene and pharmaceutical compositions thereof. The invention is also directed to a process for preparation of the salts.
US8815268 Oat extracts: refining, compositions and methods of use A simple and efficient method for the production of stable, clear, high-potency oat extracts is disclosed. The method employs the use of differential dissociation constants and ultrafiltration to stabilise extracts, prevent hazing, and prevent the loss of functional activity as an anti-irritant and anti-oxidant. Also disclosed are compositions of oat extracts derived from whole oat grains and oatmeal. Further disclosed are compositions of oat extracts for use in cosmetic, nutraceutical, therapeutic medical and veterinary preparations.
WO2012063514A1 Attractant for bone marrow stem cells, and method for attracting bone marrow stem cells The present invention addresses the problem of providing an attractant etc. for bone marrow stem cells capable of attracting bone marrow stem cells. An attractant etc. for bone marrow stem cells, which contains at least one type of fungus selected from a group comprising Deacetylcytochalasin C, a culture of Eupenicillium ludwigii and a culture of Talaromyces trachyspermus, is provided.
WO2010124654A1 Vascular embolus of sodium alginate microspheres comprising drug for resisting hemangioma, preparation method, and use thereof A vascular embolus of sodium alginate microspheres comprising drug for resisting hemangioma, the preparation method, and the use thereof are disclosed. Said micropheres comprise sodium alginate and drug for resisting hemangioma. The weight ratio of sodium alginate to drug for resisting hemangioma is 5:1 - 60:1, wherein said drug is selected from Pingyangmycin, Sodium Morrhuate, Urea, or Bleomycin. Said preparation method comprises: (a) preparing the solution of drug for resisting hemangioma and the solution of sodium alginate respectively; (b) mixing the solution of drug for resisting hemangioma with the solution of sodium alginate; (c) reacting the obtained solution mixture in the fixing solution through the high pressure static microsphere generating device to obtain the vascular embolus of sodium alginate microspheres.
US8110179 A water-soluble, cyclodextrin-containing linear polymer having bioactive moieties to attached a drug(s) or modified drug to the polymer covalently; cleavage under biological conditions to release the bioactive moieties; sustained release; side effect reduction; stability; nontoxic; drug polymer conjugate The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.
CA2576581A1 Substituted indole compounds, their preparation and use in medicaments The present invention relates to substituted indole compounds of general formula (I), a process for their preparation, medicaments comprising substituted indole compounds as well as the use of substituted indole compounds for the preparation of medicaments, which are suitable e.g. for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.
EP1599196A2 Combination therapies for the treatment of cancer Lonidamine or a lonidamine analog is administered with one or more additional anti-cancer agents or surgery or radiation to treat cancer or is administered alone or in combination to treat cancer, optionally in a sustained release formulation, and improve patient outcome.
US6911320 Pituitary tumor transforming gene (PTTG), formerly pituitary tumor specific gene (PTTG) Polypeptides are expressed by the pituitary-tumor-transforming-gene (PTTG), formerly known as pituitary-tumor-specific-gene (PTTG), and nucleic acids encode them. Examples are the human and rat PTTG proteins. The nucleic acids may be applied to the production of a recombinant protein, and to the detection of the presence of PTTG genes in different species. The nucleic acids may be operatively linked to a vector, optionally provided with control and expression sequences and/or being carried by a host cell. The nucleic acids may also be delivered to a mammal to compensate for the absence, or a defective expression, of endogenous protein. The nucleic acids, proteins, and antibodies are also employed in disgnostic assays, as well as, for example, in the production of anti-PTTG antibodies (protein), therapeutic compositions and other applications of the proteins and antibodies. Various kits utilize nucleic acids, polypeptides, and/or antibodies. A transgenic non-human mammal expresses PTTG.
EP2164499A1 Treatment of tardive dyskinesia with pyridoxal 5'-phosphate Abstract This invention relates to treatment of Tardive Dyskinesia through the administration of pyridoxal 5'-phosphate. The treatment may be an oral administration of 100 - 4000 mg/day, for example, 100-750 mg/day or about 250 mg/day. Also provided is the use of pyridoxal 5'-phosphate for the preparation of a medicament for the treatment of tardive dyskinesia, kits comprising pyridoxal 5'-phosphate for the treatment of tardive dyskinesia, and combination drugs for the treatment of tardive dyskinesia.
WO2012089607A1 Novel compounds with a 3a-azabicyclo [4.1.0] heptane core acting on orexin receptors This invention relates to azabicyclo[4.1.0]hept-4-yl derivatives and their use as pharmaceuticals.
US20120189671 Absorbable Implants and Methods for their use in Hemostasis The invention provides body absorable, mechanically hemostatic putty compositions comprising carboxymethyl cellulose and one or more of polyhydroxy compounds, fatty acids, and esters thereof for use in controlling the bleeding of bone.
CN102382097A Aromatic methylamine derivative and pharmaceutical composition, preparation method and application thereof The invention relates to an aromatic methylamine derivative as shown in formula I and medicinal salts thereof, wherein each independently represents a double bond or a single bond; R1 and R2 independently represent hydrogen, a hydroxyl, or an alkoxy respectively, or R1 and R2 are connected with a methylenedioxy; R3 and R4 independently represent hydrogen, a hydroxyl, or an alkoxy respectively, orR3 and R4 are connected with a methylenedioxy; R5 represents hydrogen, halogen, an unsaturated alkyl or a saturated alkyl; R6 represents oxygen, a hydroxyl, or an amino; R7 represents hydrogen, oxygen or sulfur. The invention also provides a preparation method of the aromatic methylamine derivative shown in formula I, and an application in preparation of medicaments for preventing or treating benign tumors or cancers.
CN101367799A Matrine salviol acid B complex salt and kuh-seng native salviol acid B complex salt, preparation method and application thereof The present invention discloses sophocarpidine salvianolic acid B complex salt, oxymatrine salvianolic acid B complex salt, preparation methods and applications thereof. The compounds can be used for preparing medicine which is used for treating liver diseases and heart cerebrovascular diseases.
EP1539142A2 Use of an amyloid beta vaccination in combination with a selective cox-2 inhibitor for the treatment of alzheimer s disease The present invention provides compositions and methods for the treatment or prevention of Alzheimer's disease. More particularly, the invention provides a combination therapy for the treatment or prevention of Alzheimer's disease, wherein the therapy comprises administering to a subject an amyloid beta vaccine in combination with a cyclooxygenase-2 selective inhibitor.
US20100178342 Solid Pharmaceutical Preparation The invention relates to a solid pharmaceutical preparation containing one or more solid carriers and/or excipients and an active substance selected from among the Monoamine Neurotransmitter Re-uptake Inhibitors which have a 2,3-disubstituted tropane structure, the preparation thereof and use thereof for preparing a pharmaceutical composition for the treatment or prevention of central-nervous diseases or disorders.
WO2013082656A1 Cage amine ligands for metallo-radiopharmaceuticals The present invention relates to compounds that are useful as metal ligands and which can be bound to a biological entity such as a molecular recognition moiety and methods of making these compounds. Once the compounds that are bound to a biological entity are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.
US8420629 Azetidine and cyclobutane derivatives as JAK inhibitors The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
CN103356656A Application of Chukrasone A in preparing medicines for treating Alzheimer disease The invention discloses a novel use of Chukrasone A, wherein the Chukrasone A has acetylcholin esterase inhibiting activity and nerve cell protective effect. The Chukrasone A as a multiple-effect target compound can be used for preparing medicines for treating alzheimer disease. The use of the Chukrasone A in preparing medicines for treating Alzheimer disease provided by the invention is disclosed for the first time. As the framework type belongs to a brand-new framework type, and the acetylcholin esterase inhibiting activity of the Chukrasone A is unimaginably strong, the probability of giving any enlightenment by other compounds does not exist. The Chukrasone A has remarkable substantial characteristics and meanwhile has remarkable progress for treating Alzheimer disease.
US20080269226 Methods for Preserving Renal Function Using Xanthine Oxidoreductase Inhibitors The present invention relates to methods of preserving renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof.
WO2011051966A3 Pharmaceutical compositions for treatment/prophylaxis of non-alcoholic fatty liver disease Disclosed herein is a novel synergistic pharmaceutical composition comprising hydroxychloroquine with insulin sensitizing agents and lipid lowering agents such as statins along with pharmaceutical excipients/carriers useful in treating Non-Alcoholic Fatty Liver Disease.
US7179804 Tachykinin receptor antagonists The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins
CN102846841A Tibetan medicine for treating AIDS The invention discloses a Tibetan medicine for treating AIDS. The Tibetan medicine is composed of active components or the active components and pharmaceutically acceptable auxiliary materials, wherein the active components are prepared by red metal ash, henbane paste, shiny-leaved yellowhorn wood paste, Tibetan codonopsis pilosula, berberis thunbergii skin, fructus podophylli and benzoin according to certain weight proportion. The Tibetan medicine is prepared into any commonly-used oral administration agent. The Tibetan medicine has effects of clearing away heat and toxic materials, resolving hard lumps, removing detumescence and strengthening the body resistance. The Tibetan medicine is mainly used for treating chronic illness, air kuning, AIDS, lymph disease and eleven inside and outside abdomen lumps named by Tibetan doctors. The Tibetan doctors consider that a root of all chronic illness is caused by indigestion, and the chronic illness cannot be caused by digestion.
EP1096926B1 Methods and compounds for treating depression The present invention features compounds active at both the serotonin euptake site and the N-methyl-D-aspartate (NMDA) receptor and the use of such compounds for treating different disorders. Compounds having activity at the serotonin reuptake site and the NMDA receptor ('multi-active compounds') can be used to treat different types of disorders such as depression, obsessive-compulsive disorders (OCD), sleep disorders, sexual dysfunction, and eating disorders. Preferably, the multi-active compounds are used to treat depression.
US20110236510 Pregnane glycoside compositions and caralluma extract products and uses thereof Pregnane glycoside or a Caralluma extract including the pregnane glycoside of the present invention can be used for medical purposes and as food additives, such as a treatment of obesity, a reduction of blood glucose, a reduction of blood pressure, a reduction in hip, waist and arm circumferences, a reduction of fat, increase of BMR, a decrease of BMI, an increase of lean body mass, an appetite-suppression and a reduction/elimination of joint pain, anti-aging, a treatment for falling sex drive, the treatment for impotency and an erectile dysfunction, and an enhancement of energy levels.
US20080057076 Novel fibroblast growth factors Novel nucleic acids, polypeptide sequences, and nucleic acid regulators thereof, have been identified which code for a fibroblast growth factor (FGF), preferably FGF-20 or FGF-23, a class of polypeptides involved in development, differentiation, and morphogenesis, e.g., in cell-cell signalling and cell proliferation. An FGF of the present invention, fragments thereof, and derivatives thereof, have one or more of the following biological activities, e.g., promoting wound healing; promoting neuronal survival; stimulating cell proliferation, e.g., proliferation of stem cells, fibroblasts, neurons, glia, oligodendrocytes, Schwann cells, or progenitors thereof; modulating differentiation of cells; inducing embryonic development; stimulating neurite outgrowth; enhancing recovery from nerve or neuronal damage; stimulating myelination; stimulating angiogenesis; receptor binding activity; modulating tumorigenesis, etc.
CN101152204A Vein drug administration preparations of clofarabine and method for preparing the same The invention provides a clofarabine intravenous injection or clofarabine medicine salt intravenous injection and the preparation method. The excipient of the injection formula is mainly sodium chloride or glucose. The injection has high thermal stability and is used to treat child refractory and recurrent acute lymphoblastic leukemia.
CN102008475A Application of quinolizidine in preparing tumor treatment drugs The invention relates to application of quinolizidine comprising sparteine and cytisine extracted from Sophora plants in preparing tumor treatment drugs. The quinolizidine can be used for treating tumors including leukemia, lymphoma, cancer of the liver, cancer of the esophagus and lung cancer. A combined medical auxiliary material including therapy effective dose of active components: sparteine and cytisine is utilized to prepare clinically applied dosage forms like injections, tablets, capsules, release-controlled pills and the like.
EP1171136B1 Immunomodulating compositions comprising urea derivatives for use in the treatment of inflammatory diseases The invention relates to immunomodulatory compositions and related methods. The immunomodulatory compositions of a formula disclosed herein are useful for the prevention of sepsis and the treatment and prevention of diseases associated with inflammation and/or NOS.
WO2009091324A1 Quinoline, naphthalene and conformationally constrained quinoline or naphthalene derivates as anti-mycobacterial agents The invention relates to a compound of general formula I, II, III, IV, V, VI, VII, VIII, IX, X or a tautomer and the stereochemically isomeric forms thereof or pharmaceutically acceptable salts thereof, a N-oxide form thereof or a pro-drug thereof. The compound is usable as a medicament for the treatment of mycobacterial disease.
US20050026983 Imidazole compounds and uses thereof Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the activation of the cannabinoid receptors in animals are described herein.
WO2008108735A1 2 -substituted- 3 -phenylpropionic acid derivatives and their use in the treatment of inflammatory bowel disease The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl) propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl) propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methylor ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.
US20100136029 Use of Tri-Substituted Glycerol Compounds for the Treatment of Hematological Malignancies The present invention relates to the use of a tri-substituted glycerol compound for the manufacture of a medicament for the treatment of hematological malignancies. The invention also refers to a kit-of-parts comprising such a medicament. Finally, the invention also relates to a corresponding method for the treatment of such conditions as well as to an in vitro method for determining the susceptibility of such malignant cells to a medicament as defined in the invention.
WO2013181217A2 Novel compounds and compositions for treatment of breathing control disorders or diseases The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention.
WO2009047537A1 Preparation for treating intestinal infection comprising oligosaccharides and insoluble cellular material A preparation for use in the treatment of Clostridium difficile or salmonella infection comprising a mixture of galacto-oligosaccharide and matter from cranberry.
WO2006035617A1 α2 RECEPTOR BLOCKING AGENT CONTAINING INDOLE DERIVATIVE AS ACTIVE INGREDIENT AND VASODILATOR A compound having a simpler structure than yohimbine, which is a pentacyclic fused heterocyclic compound, and having an activity similar to that of yohimbine. Also provided is an α2 receptor blocking medicine or food composition containing either a compound represented by the formula : [Chemical formula 1] (X) (wherein R1 represents hydrogen, alkyl, alkenyl, alkynyl, an aromatic group, aralkyl, acyl, arylsulfonyl, alkylsulfonyl, or hydroxy; R2 represents a hydrocarbon group; R3, R4, R5, R6, and R7 are the same or different and each represents hydrogen, halogeno, alkyl, or alkoxy; R8 represents hydrogen or acyl; n is an integer of 1-6; and a and b are the same or different and each is 1 or 0) or a pharmaceutically acceptable salt thereof.
US20060089337 Estrogen replacement regimen The present invention provides an improved method to deliver estrogen to menopausal women comprising administering ultra-low dose estradiol alternating with standard-dose estradiol.
CN101991566A Application of lariciresinol to preparing medicament for resisting autoimmune disease and graft rejection disease The invention provides application of lariciresinol to preparing a medicament for resisting an autoimmune disease and a graft rejection disease. An experiment discovers that: the lariciresinol can inhibit human dendritic cell proliferation in vitro and inhibit the capability of human dendritic cells of promoting allogeneic T cell proliferation reaction and enhancing the secretion of interleukin 10. Meanwhile, in an experimental autoimmune myelomeningitis model, the lariciresinol is applied in vivo, so that an average clinical score of mice can be reduced and the spinal infiltration of mononuclear cells is inhibited. In a heart transplant experiment, the lariciresinol is applied in vivo, so that the survival time of a transplanted heart is prolonged. In a delayed hypersensitivity model, the lariciresinol is applied in vivo, so that the auricle swelling degree of the mice can be reduced. In-vivo and in-vitro results both show that: the lariciresinol has the certain effect of resisting the autoimmune disease and graft rejection disease. The medicament is a preparation which consists of the lariciresinol serving as an active ingredient and a medical carrier, and comprises an oral preparation, an injection, a suppository, an external preparation and the like.
CN103356596A Application of Chukrasone B in preparation medicines for treating influenza virus A The invention discloses an application of Chukrasone B in preparation of medicines for treating influenza virus A. Experiments prove that the Chukrasone B has remarkable inhibiting effect to influenza virus A, so that the Chukrasone B has potential application value in the field of treatment of infectious diseases such as influenza virus A. The application of the Chukrasone B in preparation of medicines for treating influenza virus infection provided by the invention is disclosed for the first time. As the framework type is a brand new framework type and the inhibitory activity of the Chukrasone B to influenza virus is unimaginably strong, the probability of giving any enlightenment by other compounds does not exist. The Chukrasone B has remarkable substantial characteristics and meanwhile has remarkable progress in treatment of influenza virus infection.
US7125687 Presenilin enhancers assays The invention provides methods and compositions relating to pen polypeptides having pen-specific structure and activity, related polynucleotides and modulators of pen function. The invention provides isolated pen hybridization probes and primers capable of specifically hybridizing with natural pen genes, pen-specific binding agents such as specific antibodies, and methods of making and using the subject compositions in diagnosis (e.g. genetic hybridization screens for pen transcripts), therapy (e.g. pen inhibitors to modulate APP processing) and in the biopharmaceutical industry (e.g. as immunogens, reagents for screening chemical libraries for lead pharmacological agents, etc.).
WO2007070393A3 Mglur1 anatgonists as therapeutic agents In its many embodiments, the present invention provides tricyclic compounds of formula (I) (wherein J1 - J4, X, and R1- R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
CN101019850A Externally applied aceclofenac gel prepn and its prepn process The present invention discloses one kind of externally applied aceclofenac gel preparation and its preparation process. The externally applied aceclofenac gel preparation is compounded with aceclofenac 0.5-8 wt%, organic solvent 5-50 wt%, bacteriostat 0.001-10 wt%, pH regulator 0.01-2 wt%, carbomer 0.5-8 wt%, antioxidant 0.01-5 wt% and water for the rest. It is prepared through mixing the said ingredients. It is applied to the joint or other disease focus to result in obvious curative effect.
CN101328475A Nucleic acid molecule NRN1SR11 and use thereof in anti-cancer medicine preparation The invention belongs to the biomedical field and relates to NRN1SR1 and an application of the NRN1SR1 in the preparation of an antitumor drug. The tumor threatens the health of people. The invention provides the nucleotide molecule NRN1SR1 used for preparing the antitumor drug, and the sequence comprises 5'-GGCAGCUUAUUCGAACUCU-3' or 5'- GGCAGCTTATTCGAACTCT-3'. Compared with nude mice without the NRN1SR1 in the same culture condition, the nude mice containing the NRN1SR1 has a tumor body prevented from growing evidently; moreover, the phenomenon is more evident as time goes on. The product provides a novel way and method for treating and relieving the tumor.
US20110135684 Use of L-alpha-lysophosphatidylcholine to obtain the differentiation of monocytes in mature dendritic cells in vitro A method for treating and/or preventing certain ailments by administering to a person in need thereof L-α-lysophosphatidylcholine as an agent for activating the immune system of the person. Also, vaccine compositions that include L-α-lysophosphatidylcholine.
US20090318465 Method for identifying compounds that act as insulin-sensitizers The present invention relates to a method for identifying compounds that act as insulin-sensitizers. The method can include screening of test compounds in two assays of insulin sensitivity. This method can identify lead compounds for the treatment of disorders caused by insulin resistance to glucose uptake. This invention also includes methods for treating insulin resistance and related disorders.
DE102005018184A1 New phenyl ester compounds useful as antioxidants, for the reduction of skin aging, or for the prevention/treatment of inflammations, allergies and irritations of skin Phenyl ester compounds (I) are new. Phenyl ester compounds of formula (I) are new. R1>H, 1-30C alkyl, 1-30C hydroxyalkyl; X : CN, -C(=O)-R1> or -C(=O)-OR1>; Y1>H or Ar, where Ar is benzene compound of formula (a); and R2>-R6>H, OH, 1-20C alkoxy, 1-20C alkyl, 3-20C alkenyl, 1-20C hydroxyalkyl (where the hydroxy group is bound to a primary or secondary carbon atom of the chain and the alkyl chain is interrupted by O), or 1-20C hydroxyalkoxy (where the hydroxy group is bounded at primary or secondary carbon atoms of the chain and the alkyl chain is interrupted by O), where one of R2>-R6> is 1-20C alkoxy or 2-20C alkylenoxy-spacer, which is bound over Si-atom at oligo- or polysiloxane chain. Independent claims are included for: (1) a composition comprising (I) and at least one cosmetic or dermatological composition or household product suitable carrier; and (2) the preparation of (I). [Image] - ACTIVITY : Dermatological; Antiinflammatory; Antiallergic; Cytostatic. - MECHANISM OF ACTION : None given.
US20120301449 Rna interference target for treating aids The RNAi target sequences, which could be used for treating AIDS through targeting HIV. Based on the target sequences, recombinant expression vectors, packaging vectors and cells were constructed, which express siRNA and/or miRNA and/or ribozyme and/or antisense oligonucleotide for targeting HIV. And the applications of said recombinant expression vectors, packaging vectors and cells in preparing medicament for treating AIDS.
US20080206348 Cilostazol-Containing Pharmaceutical Composition Based On Particles Of Less Than 50 Micrometers The present invention relates to cilostazol compositions, process for their preparation, and methods for their administration to treat a condition. In the cilostazol compositions, 90% of the cilostazol particles have a particle size less than about 50 μm.
WO2013174930A3 7-oxo-thiazolopyridine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease The present invention relates to a compound having the general formula (A), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diasiereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
CN103230589A Fibrinogen compound and application thereof The invention discloses a fibrinogen compound and an application thereof. The fibrinogen compound comprises fibrinogen, prothrombin and eleven neurotrophic factors. The fibrinogen compound can be used for preparing drugs for treating glaucoma, hypophysoma, traumatic optic nerve injury, operation caused optic nerve injury and the like; and when the compound is combined with transplanted cells, the transplanting repair effect can be enhanced.
US20080032920 Macromolecules modified with electrophilic groups and methods of making and using thereof Described herein are macromolecules modified with electrophilic groups and methods of making and using thereof. The preparation of a thiol-reactive, electrophililic derivative of HA in order to prepare “crosslinker-free” hydrogels are described as well as compounds and methods that are capable of coupling two or more molecules, such as macromolecules, under mild conditions. Specifically disclosed is the introduction of reactive bromo- and iodoacetate functionalities at the hydroxyl groups that are abundantly present on the HA polymer. The “crosslinker-free” hydrogels described have numerous applications including, but not limited to, drug delivery, small molecule delivery, wound healing, burn injury healing, tissue regeneration/engineering, cell culturing, and bio-artificial materials.
CN103405747A Preparation method for alanyl-glutamine biological adhesive preparation as well as product and application of preparation The invention aims at disclosing a preparation method for an alanyl-glutamine biological adhesive preparation as well as a product and an application of the preparation. The alanyl-glutamine biological adhesive preparation is a topical gel preparation taking alanyl-glutamine as a main medicine ingredient for dental ulcer; the preparation has the characteristics of being capable of rapidly alleviating the pain of the affected parts, definite in curative effect, capable of being adhered to the surface of ulcer for a long time to protect the surface of a wound and slowly releasing medicines, less in irritation, good in biocompatibility, capable of integrating dental ulcer treatment, immune adjustment and recurrence prevention, convenient for patients to use, easy to carry and store, and low in price.
CN103656454A Medicine for treating children infantile malnutrition and preparation method thereof The invention discloses a medicine for treating the children infantile malnutrition and a preparation method thereof. The medicine is mainly prepared from lychee seeds, hawthorns, borneol, rhizoma sparganii, fruit of rangoon creeper, atractylodes macrocephala and other medical materials according to a certain weight ratio. The medicine provided by the invention has the functions of repelling foulness, clearing damp, moistening dryness and realizing detoxification, is high in efficiency when being used to treat the children infantile malnutrition and good in curative effect, and causes no toxic or side effects.
US20090105172 Stabilized Aptamers to PSMA and Their Use as Prostate Cancer Therapeutics The present invention provides stabilized, high affinity nucleic acid ligands to PSMA. Methods for the identification and preparation of novel, stable, high affinity ligands to PSMA using the SELEX™ method with 2′-O-methyl substituted nucleic acids, and cell surface SELEX™ are described herein. Also included are methods and compositions for the treatment and diagnosis of disease characterized by PSMA expression, using the described nucleic acid ligands.
CN101518638A Pearl pill and method for preparing same The invention relates to a pearl pill and a method for preparing the same, in particular to a process for preparing a novel pearl pill according to a 25-ingredient pearl pill which is traditional Tibetan medicine. The superfine pulverizing technology is adopted in the process for preparing the compound medicine to pulverize raw material to superfine powder of 0.01-50 micrometers and conventional auxiliary material is added to the superfine powder so that various pills are prepared according to the conventional process. Experiments prove that the process for preparing the compound medicine is improved without changing main treating functions of the pearl pill so that a novel pearl pill is prepared, difficult process problems that the traditional pearl pills have coarse surfaces, large difference in weight, poor disintegration, superstandard water content, superstandard microorganism, and the like are solved, the period of the bath production of the pearl pill is shortened, relatively lower cost and high degrees of industrialization and mechanization are achieved, the requirement of modern pharmaceutical technology is satisfied, and the invention is adapted to the life style of modern people.
US20060088580 Hormone-containing transdermal therapeutic system with an active substance reservoir based on vinylacetate-vinylpyrrolidone copolymer with improved cohesion A transdermal therapeutic system in patch form for the controlled delivery of active substances to the human or animal skin comprises a backing layer, an active substance-containing reservoir attached thereto and a detachable protective layer, is characterized in that the active substance-containing reservoir contains as main components thereof at least one film former as well as at least one polymer which prevents or suppresses the crystallisation of the active substance or active substances.
WO2008074068A1 Substituted quinoline derivatives as antiamyloidogeneic agents The present invention relates to heterocyclic compounds, processes for their preparation and their use as pharmaceutical or veterinary agents, in particular for the treatment, amelioration and/or prophylaxis of conditions caused by or associated with unbalanced metal levels and/or oxidative stress, such as neurological conditions and cellular proliferative disorders, for example Alzheimer's disease, Parkinson's disease, Huntington's disease or brain cancer or tumours.
EP2211851A2 Laminins, derivatives, and compositions including same and method for their therapeutic use In various embodiments, the present disclosure provides a method of treating a subject using laminin or a composition that includes laminin. In one embodiment, the method is used to enhance muscle regeneration, maintenance, or repair in a subject. In another embodiment, the method is used to promote wound healing. The method, in yet another embodiment, is used to prevent or reduce muscle damage or injury. In specific implementations of these methods, the laminin or composition that includes laminin is administered in a therapeutically effective amount. In some implementations, the laminin is a complete laminin protein. In other implementations, the laminin is a laminin fragment, a laminin derivative, or a laminin analogue.
CN103211810A Application of Oroxylin A The invention discloses application of Oroxylin A in preparation of medicines for promoting liver regeneration. Experiments show that Oroxylin A can effectively protect liver, improve liver regeneration by means of improving expression level of IL-1Ra and TNF-alpha of liver cells, and promote the reshaping of the liver structure and is beneficial to restore of liver function. Experiments show that the survival rate of mice with liver injury in experimental group can be remarkably improved by Oroxylin A.
CN103099791A Oral composition of meloxicam capable of increasing dissolution rate The invention relates to the field of a pharmaceutical preparation, and in particular relates to a meloxicam oral preparation capable of increasing a dissolution rate and a preparation method of the preparation. The oral composition is characterized by mainly consisting of 1 part of meloxicam, 0.02-0.047 part of a solubilizer, 0.20-0.40 part of an adhesive, 3.33-4.67 parts of a filling agent, 0.013-0.08 part of a lubricant, and 0.33-1.33 parts of a disintegrating agent. The preparation disclosed by the invention improves the dissolution rate of medicine and enhances clinical effect.
US20110262521 Medical device including bacterial cellulose reinforced by resorbable or non resorbable reinforcing materials The present invention relates to a medical device comprising: a reinforcing member; and bacterial cellulose on at least a portion of the reinforcing member. The invention also relates to a method for making such a medical device.
CN103408571A Crystal form I of rifabutin, and preparation method and application thereof The invention belongs to the field of chemical medicines, and in particular relates to a crystal form I of rifabutin, and a preparation method and application thereof, for solving the problem that the existing amorphous rifabutin is bad in mobility and poor in stability. According to the technical scheme, the crystal form I of rifabutin is used for solving the problems of the existing amorphous rifabutin. The invention further provides the preparation method and application of the crystal form I of rifabutin. The mobility and the stability of the crystal form I of rifabutin provided by the invention are superior to those of amorphous rifabutin; content uniformity and medication safety of rifabutin capsule preparation production are ensured; in addition, bulk drugs and preparations can have longer validity periods.
US20110184058 Synthesis of 6,7-dihydro-1h-indeno[5, 4-b] furan-8(2h)-one as intermediate in the preparation of remelteon The present invention describes the preparation of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one, a key intermediate in preparation of ramelteon. The present invention also describes further preceding intermediate compounds useful for the synthesis of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one.
WO2008139938A1 Double-stranded nucleic acid molecule targeting for human papilloma virus type-16 gene, and pharmaceutical agent comprising the molecule Disclosed are: a double-stranded nucleic acid molecule (e.g., siRNA) which has a high inhibitory activity on and a high specificity to the expression of human papilloma virus (HPV) type-16 oncogene; and a pharmaceutical agent or the like which is suitable for the treatment or prevention of a disease (e.g., cervical cancer) induced by the infection with HPV type-16. Specifically disclosed are: a double-stranded nucleic acid molecule which targets for a specific sequence located in each of HPV type-16 E6 and E7 oncogenes and which has a high inhibitory activity on and a high specificity to the expression of the gene; and DNA, a vector and a pharmaceutical agent comprising the double-stranded nucleic acid molecule.
CN103385919A Anti-inflammatory drug for postpartum sow and preparation method thereof The invention discloses an anti-inflammatory drug for a postpartum sow and a preparation method thereof. The preparation method comprises the following steps of crushing 9-11% of naproxen and 28-32% of metronidazole, sieving the crushed naproxen and metronidazole to obtain naproxen and metronidazole of 100 meshes, pouring 9-11% of the crushed naproxen, 28-32% of the crushed metronidazole, 1.8-2.2% of gentamycin sulfate, 1.0-1.4% of metoclopramide, 17.4-17.8% of motherwort, 27.36-27.40% of pottery clay and 9-11% of Daditian into a wet granulation machine, carrying out uniform mixing, adding 1.80-1.84% of starch into the mixture, carrying out stirring for 8min, pouring the stirred mixture into an oscillating granulator, carrying out granulation, feeding the granules into a fluidized bed by a negative pressure pipe, carrying out drying, and carrying out sieving and packaging.
EP1650312A2 Functional assay of high-density lipoprotein A kit for evaluating the risk of atherosclerosis in a mammal, said kit comprising a container containing one or more oxidised or non-oxidized phospholipids, and instructional materials describing the following assay for evaluating the risk of atherosclerosis in a mammal: (A) contacting a high density lipoprotein (HDL) comprised in a biological sample from said mammal with an oxidised phospholipid; and measuring a change in the amount of oxidised or non-oxidised phospholipid wherein the absence of change in the amount of oxidised phospholipid indicates the mammal is at risk of atherosclerosis or (B) contacting a high density lipoprotein (HDL) comprised in a biological sample from said mammal with a phospholipid; subjecting the phospholipid to oxidising conditions; and measuring a change in the amount of oxidised or non-oxidised phospholipid wherein a change in the amount of oxidised or non-oxidised phospholipid indicates the mammal is at risk for atherosclerosis
WO2009156860A3 4-(pyridin-4-yl)-1h-(1, 3, 5)triazin-2-one derivatives as gsk3-beta inhibitors for the treatment of neurodegenerative diseases A triazinone derivative represented by formula (I) wherein: Z represents a bond, a carbonyl group, a methylene group optionally substituted by one or two groups chosen from a C1-6 alkyl group, a hydroxyl group, a Ci-β alkoxy group; R1 represents a 4-pyridine ring; R2 represents a hydrogen atom, a C1-6 alkyl; R3 represents a hydrogen atom, a C1-6 alkyl group; R2 and R3 may form together a 6 membered cycle with the nitrogens caring R2 and R3 optionally substituted; R4 represents: a phenyl ring, being optionally substituted; n represents 0 to 2; in form of a free base or of an addition salt with an acid. The compounds of the present invention have GSK3β inhibitory activity and are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activity of GSK3β and more particularly of neurodegenerative diseases.
CN101536980A Rubescensin preparation and preparation method and use of same The invention generally relates to a diterpene pharmaceutical preparation and preparation method and use of the same. Particularly, the invention discloses a pharmaceutical preparation, which comprises diterpenes such as the rubescensin and amphiphilic surfactants, and any other pharmaceutically acceptable carriers and/or excipients. In addition, the invention also relates to the preparation method and the use of the pharmaceutical preparation in disease treatment.
WO2006078842A1 Use of methylnaltrexone and related compounds to treat post-operative gastrointestinal dysfunction Methods and compositions for treating post-surgical gastrointestinal dysfunction are provided. Methods include administering a quaternary derivative of noroxymorphone (e.g., methylnaltrexone) to a patient after a segmental colectomy is performed on the patient.
CN103242210A Mulin acetate containing substituted squaric acid and application thereof The invention relates to Mulin acetate containing substituted squaric acid and an application thereof which belong to the technical field of medicines, specifically to substituted squaric acid containing Mulin acetate as shown in a general formula (I), pharmaceutically acceptable salt, a hydrate and an isomer thereof, wherein R1, R2, R3, R4, R5 and B are defined in the specification. The invention also relates to a preparation method of these compounds, a pharmaceutical composition containing these compounds and an application of these compounds in the preparation of drugs for treating or preventing bacteria and virus. As for staphylococcus aureus and Streptococcus equin MIC value, the compounds have an antibacterial effect 15-20 times higher than a control commercially-available antibiotic tiamulin in the test. And the compounds provided by the invention are effective antimicrobial agents. And the compounds provided by the invention are effective antimicrobial agents.
CN103040926A Multi-purpose anti-itch cream The invention relates to a multi-purpose anti-itch cream which is prepared from glycerin, triethanolamine, borneol, camphor, radix sophorae flavescentis, dual glycerol stearate, liquid paraffin and methyl salicylate through an emulsification technology. The anti-itch cream has extremely strong antipruritic, sterilizing, anti-inflammatory and analgesic efficacies, can be used for insect-biting dermatitis, itchy skin, contact dermatitis, eczema and other skin inflammation, is good in affinity with skin and hair, and is mild, non-irritating, safe, and free of toxic and side effects.
CA2696009A1 Antiviral composition comprising a sulfated polysaccharide The present invention provides for the use of iota- and/or kappa-carrageenan for the manufacture of an antiviral pharmaceutical composition for the prophylaxis or treatment of a pathological condition or disease caused by or associated with an infection by a respiratory virus selected from the group consisting of orthomyxovirus, paramyxovirus, adenovirus and coronavirus. The present invention further provides for the use of fucoidan, in particular of high molecular weight fucoidan, for the manufacture of an antiviral pharmaceutical composition for the prophylaxis or treatment of a pathological condition or disease caused by or associated with an infection by a respiratory virus selected from the group consisting of orthomyxovirus and paramyxovirus.
WO2010149772A1 Preparation comprising insulin, nicotinamide and an amino acid Insulin preparations comprising an insulin compound or a mixture of two or more insulin compounds, a nicotinic compound and an amino acid.
US20120214775 Pharmaceutical Salts of 3-O-(3',3'-Dimethylsuccinyl) Betulinic Acid Salts of 3-O-(3′,3′-dimethylsuccinyl)Betulinic acid (DSB) are disclosed. Particularly, the preparation, pharmaceutical evaluation, and in vivo bioavailability evaluation of N-methyl-D-glucamine and alkali metal salt forms of DSB are disclosed. Pharmaceutical compositions including these salt forms are used in methods of treating HIV and related diseases. Methods of making the salts of DSB and the pharmaceutical compositions are also provided.
CN103169690A Application of complex of parietic acid or parietic acid compounds and arginine in preparation of medicines for treating vascular complications of diabetes The invention relates to application of complex of parietic acid or parietic acid compounds and arginine in preparation of medicines for treating vascular complications of diabetes. The vascular complications of diabetes mean diabetic great vascular complications or diabetic microangiopathy and comprise diabetic testopathy, sexual debility of diabetic complications (comprising diabetic testopathy and diabetic impotence), diabetic retinopathy and diabetic neuropathy. The complex is abbreviated as Dajingsuan which is a novel crystallized compound and enters into body to release parietic acid and arginine; the solubility of parietic acid is changed, so that the bioavailability is improved and the stability is good. A novel structural characteristic is endowed to a parent compound of parietic acid; Dajingsuan enters into body to release parietic acid and arginine, so that the function of parietic acid which inhibits inflammatory factors: NFkB, TNF alpha, ROS, EGF and the like to regulate the endothelin system is exerted.
CN103637988A Preparation method for curcumin long circulating liposomes Provided is a preparation method for curcumin long circulating liposomes. The method comprises steps: curcumin, soybean lecithin, cholesterol and polyethylene glycol- distearoyl phosphatidyl ethanolamine are weighed in a mass ratio of 1:30-50:3-5:1-3; the above raw materials are dissolved in ethanol as an organic phase; a phosphate buffer salt solution with a pH value of 6-7 is taken as an aqueous phase; under a rotating speed of 1000-1500 r/min, the organic phase is dropwisely added in the organic phase with thermal insulation at the temperature of 40-50 DEG C slowly and at a constant speed; after the dropwise add, stirring is continued for 2-3h, the organic solvent is volatilized, and a solution of the curcumin long circulating liposomes is obtained. The beneficial effects of the preparation method are mainly that, Cur-LCL is prepared through ethanol injection method, the technology is simple, the entrapment rate is high, the particle sizes are small, the release in vitro is slow, and the in vivo pharmacokinetics data display that the plasma clearance is decreased obviously, the half-life period is remarkably prolonged, and the curcumin long circulating liposomes have certain long circulation effects.
WO2008018827A1 Benzimidazole derivatives useful in treatment of vallinoid receptor trpv1 related disorders The claimed invention provides benzimidazole derivatives antagonists of VR1, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds of Formula I may be used in the treatment of osteoarthritis, chronic tendinitis, pelvic pain and peripheral neuropathy, gastroesophageal reflux disease, irritable bowel syndrome and overactive bladder.
CN1615896A Medicine for regulating blood fat and treating cardiocerehral disease and preparing method The present invention relates to a kind of medicine prepared with effective components extracted from natural plant medicine materials and for treating cardiac and cerebral vascular diseases and its preparation process. The medicine consists of gensenoside Rb3 in 1-90 wt% and medicinal supplementary material the rest. The medicine is prepared into tablet, coated tablet, oral controlled release preparation, capsule, etc. and is used in treating hyperlipemia, atherosclerosis, coronary heart disease and other cardiac and cerebral vascular diseases.
CN101584693A Pralidoxime chloride-containing drug composition and method for preparing same The invention relates to the technical field of medicaments, in particular to a pralidoxime chloride-containing medicinal composition and a method for preparing the same. The medicinal composition solves the problems of poor stability, short expiry date and the like existing in similar medicaments sold in the present markets, and has the characteristics of high stability, small drug-using volume, and convenient storage and transportation.
US8399469 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.
US20080261981 3-{4-[4-(2-amino-3-morpholin-4-yl-3-oxo-propyl)-phenoxy]-phenyl}-N-hydroxypropionamide hydrochloride; for reducing blood glucose, free fatty acids, cholesterol, triglycerides levels Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treating related disorders such as body weight gain, elevated free fatty acid, cholesterol and triglyceride levels and other disorder exacerbated by obesity.
US20100113493 (pyrrolidin-2-yl)phenyl derivatives The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein R1 is (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, or halo(C1-4)alkyloxy; R2 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; R3 is H, (C1-4)alkyl or halo(C1-4)alkyl; R4 is H, (C1-4)alkyl or halo(C1-4)alkyl; R5 is H, (C1-4)alkyl or halo-(C1-4)-alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C3-6)cycloalkyl group, optionally substituted with halogen; R6 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
US7528252 Derivatives of triazoly-imidazopyridine useful as ligands of the adenosine A2a receptor and their use as medicaments Compounds of formula (I) wherein: X is CH or CH—R2; R1 is C1-C6 linear or branched alkyl or C1-C6 linear or branched alkenyl; R2 is hydrogen, C1-C6 linear or branched alkyl or C1-C6 linear or branched alkenyl, C6-C14 aryl or C6-C14 aryl(C1-C6) linear or branched alkyl or C6-C14 aryl(C1-C6) linear or branched alkenyl, with the aryl group optionally substituted by one or more substituents, either the same or different, selected from the group consisting of halogen, hydroxy, C1-C6 alkoxy linear or branched or C1-C6 alkenyloxy linear or branched, amino, optionally mono- or disubstituted with C1-C6 linear or branched alkyl; R3 is NH2, or NHR4; R4 is C1-C6 alkyl or C1-C6 hydroxyalkyl, C1-C3 alkoxyalkyl, amino(C1-C6)alkyl, where the amino group is optionally substituted with one or two C1-C3 linear or branched alkyl groups, or with one or two C2-C3 alkenyl groups C6-C14 aryl or C6-C14 aryl(C1-C6)alkyl, with the aryl group optionally substituted by one or more substituents, either the same or different, selected from the group consisting by halogen, hydroxy, C1-C6 alkoxy linear or branched or C1-C6 alkenyloxy linear or branched, amino, mono- or di-substituted with C1-C6 alkyl linear or branched or C1-C6 alkenyl linear or branched; and their pharmaceutically acceptable salts. These compounds are antagonists of the adenosine A2a receptor and useful as medicaments, in particular for the treatment of Parkinson's disease.
CN103356554A Application of Sarcaboside B in preparation of medicines for treating rhinitis The invention discloses Sarcaboside B for treating immune-inflammation. The Sarcaboside B is used for the preparation of medicines for treating the immune-inflammation and is particularly suitable for the preparation of medicines for treating rhinitis. Compared with tefeineidingpian and diclofenac sodium, the Sarcaboside B has a definite curative effect. The application of the Sarcaboside B in the preparation of the medicines for treating the rhinitis is disclosed by the invention for the first time. As the skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpected strong inhibitory activity on rhinitis treatment, and the possibility that other compounds provide revelation does not exist. The Sarcaboside B has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for preventing and treating the rhinitis.
US20110244039 Absorbable solid compositions for topical treatment of oral mucosal disorders The invention provides a solid, self-bioadhesive composition for topical application that adheres to the oral mucosal tissue comprising a therapeutically effective amount of at least one herbal or homeopathic active agent; and a pharmaceutically acceptable solid bioadhesive carrier in an amount from about 40 to 99 percent based on the weight of the whole composition.
WO2007104242A1 Compounds capable of inhibiting zinc ion metalloproteinases The invention has disclosed 1,2,3-trihydroxy benzene and its derivatives or pharmaceutically acceptable salts of formula I for zinc ion metal-protease inhibition. These compounds are used for selective depressants of zinc ion metal-proteases such as MT1-MMP,gelatinase A, B and collagenase, matrilysins, metal-elastase or stromelysin-1. These depressants can be used to adjust many physiological or pathology courses which are concerned with MMPs, ADAMs, ADAM-TS such as vessel rebirth, wound healing, organ transplantation, fecundation course and reactivation capability, bone rebuilding and ache. They are used for treating cancer, cardiovascular diseases, arthritis, periodontal disease, multiple sclerosis, inflammation, adenomyosis, cornea ulcer, bacterial meningitis, diabetic syndrome, kidney diseases, nerve retrogression diseases, AIDS, bleb, anaphylaxis, adenomyosis, osteoporosis, asthma and so on. These blocking agents can be used for antisenescence, antibiosis, commercial manufacture addition agents of cell epimatrix, collagen product, cosmetics and make-up preparation. They can used for animals and other living bodies.
WO2006085102A1 Combination of methylxanthine compounds and steroids to treat chronic respiratory diseases There is provided the use of a methylxanthine derivative such as theophylline and a steroid in a synergistic combination for the treatment of chronic obstructive pulmonary disease, wherein the combination is administered by the inhaled route for pulmonary delivery.
WO2009109525A1 Use of a specific pde4 inhibitor for the treatment and/or prophylaxis of non-alcoholic fatty liver disease The invention relates to the use of (2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydrophenanthridin-2-ol or a pharmaceutically acceptable salt thereof for the treatment and/or prophylaxis of non-alcoholic fatty liver disease (NAFLD).
EP2301556A1 Co-Administration of a Polysaccharide with a Chemotherapeutic Agent for the Treatment of Cancer Compositions and formulations comprising a galactomannan polysaccharide component capable of increasing cell membrane fluidity or capable of parenteral administration are disclosed. Also disclosed are uses for such compositions and formulations and suitable chemical structure and size of the galactomannan polysaccharide component.
US20120270833 Immune activation of green tea hydrolysate and method for preparing food composition containing the same Disclosed are an immune-boosting food composition containing a green tea hydrolysate as an active component, and a method for preparing the same.
WO2004080482A8 Use of angiotensin converting enzyme (ace) inhibitors to prevent diabetes in a subject with chronic heart failure The present invention relates to the effect of angiotensin-converting enzyme (ACE) inhibitors on the prevention of diabetes in a subject with left ventricular dysfunction. A retrospective study was conducted to assess the effect of the ACE inhibitor enalapril on the incidence of diabetes in a group of patients from the Montreal Heart Institute enrolled in the Studies of Left Ventricular Dysfunction (SOLVD). Clinical charts were evaluated for fasting plasma glucose (FPG) levels by blinded reviewers. A diagnosis of diabetes was made when a FPG 126 mg/dL (7 mmol/L) was found at 2 visits (follow-up, 2.9±1.0 years). Of the 291 non-diabetic patients enrolled in the SOLVD study, 153 of these were on enalapril and 138 were on placebo. Baseline characteristics were similar in the 2 groups. Forty patients developed diabetes during follow-up, 9 (5.9%) in the enalapril group and 31(22.4%) in the placebo group (P<0.0001). By multivariate analysis, enalapril remained the most powerful predictor for risk reduction of developing diabetes (hazard ratio, 0.22; 95% confidence intervals, 0.10 to 0.46; P<0.0001). Enalapril therefore significantly reduces the incidence of diabetes in patients with left ventricular dysfunction, especially those with impaired FPG.
US20070010585 Compounds having strong beta -galactosidase inhibitory activity or beta -glucosidase inhibitory activity; excellent solubility; pseudo-sugar; excellent treatment or prevention of glycolipid metabolic disorders An acid addition salt of a carba-sugar amine derivative represented by the following formula (1): wherein R1 and R2 each independently represents a hydrogen atom, or an alkyl group, an alkenyl group, an alkynyl group, an acyl group, an aryl group or an aralkyl group which may have one or at least two of the following substituent (I) or (II), or R1 and R2 are taken together to represent a substituent (III) (R8 to R12 each independently represents an alkyl group, an alkenyl group, an alkynyl group, an acyl group, an aryl group or an aralkyl group), with the proviso that both R1 and R2 are not a hydrogen atom at the same time; R3, R4 and R7 each independently represents a hydroxyl group or a hydroxyl group having a substituent; and R5 and R6 each independently represents a hydrogen atom, or a hydroxyl group or a hydroxyl group having a substituent, with the proviso that when one of R5 and R6 is a hydrogen atom, the other is a hydroxyl group or a hydroxyl group having a substituent.
US20100113411 Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions The present invention relates to CGRP antagonists of general formula wherein A, U, V, W, X and R1 to R3 are defined as in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
CN101181577B Lavender strip containing natural aromatic plant The invention relates to a lavender strip which contains natural fragrant plants, comprising 80 to 85 parts of lavender, 10 to 15 parts of citrus aurantium flower, 5 to 10 parts of pummelo flowers, 2parts of fructus amomis, 2 parts of banksian rose and 2 parts of sodium carboxymethyl cellulose. The invention is a composite, wherein, the lavender has the effects of relieving stress, preventing depress, helping sleeping, eliminating heat stroke and relaxing muscle, and the fragrance of the lavender has the effects of smoothing mood and releasing stress; the Dai Dai flower has the effects of dispersing stagnated liver qi for regulating stomach, promoting qi and relieving stagnancy; the pummelo flower has the effects of promoting the circulation of qi and relieving pain; the fructus amomi hasthe effects of eliminating dampness, dispelling cold, expelling phlegm and preventing recurrence of malaria; and the banksian rose has the effects of promoting circulation of qi and relieving pain. In addition, when matched with the well-known adjustable needle warming moxibustion apparatus, the invention can realize safe health regulation for people. Moreover, the invention can be used in skin-beautifying upkeep and health care physical therapy such as relieving stress, eliminating muscular pain, promoting circulation of qi to relieve pain, detoxifying and reducing swelling, etc; moreover, the invention has the advantages of delightful fragrance and low cost.
US20090215727 Inhibition of atp-mediated, p2x7 dependent pathways by pyridoxal-5-phosphate and vitamin b6 related compounds P5P can be used as effective treatments for the modulation of P2X7, IL-1β, and inflammation response, and for diseases in which prevention of P2X7-dependent pathways or prevention of release of IL-1β is desirable, such as epithelial cancer, leukemia, brain tumors, spinal cord injury, tuberculosis, Alzheimer's Disease, neurodegenerative diseases, autosomal recessive polycystic kidney disease, diabetes, including type I diabetes, prostate cancer, and osteoporosis, bone formation and resorption.
US7214667 Drugs against articular failure The object of the present invention is to provide a composition which exerts a higher effect on recovering health from articular disorders than that attained by amino sugars and glycosaminoglycans. The present invention solves the object by providing an agent for treating articular disorders, comprising an amino sugar and trehalose as effective ingredients.
CN103007184A Method for making health-care plaster and health-care plaster made by same The invention discloses a method for making a health-care plaster. The method comprises the following steps of: mixing astragalus root, asarum, drynaria rhizome, stauntonia hexaphylla, Szechuan lovage rhizome, safflower, malaytea scurfpea, angelica dahurica, divaricate saposhnikovia root, notopterygium root, ligusticum, clematis root, monkshood, kusnezoff monkshood root, paniculate swallowwort root, angelica pubescens, acanthopanax bark, mistletoe, root of red-rooted salvia, turmeric, bighead atractylodes rhizome, Chinese angelica, white peony root, tuber fleeceflower stem, trident maple stem, silkworm excrement, wing nut leaf, banana root, borneol, rehmannia, honey, white sugar and camellia oil as raw materials, crushing, soaking in white spirit, and thus obtaining the health-care plaster. The health-care plaster comprises astragalus root, asarum, drynaria rhizome, stauntonia hexaphylla, Szechuan lovage rhizome, safflower, malaytea scurfpea, angelica dahurica, divaricate saposhnikovia root, notopterygium root, ligusticum, clematis root, monkshood, kusnezoff monkshood root, paniculate swallowwort root, angelica pubescens, acanthopanax bark, mistletoe, root of red-rooted salvia, turmeric, bighead atractylodes rhizome, Chinese angelica, white peony root, tuber fleeceflower stem, trident maple stem, silkworm excrement, wing nut leaf, banana root, borneol, rehmannia, honey, white sugar, camellia oil and white spirit. The health-care plaster has the beneficial effects of practicability and low making cost.
CA2296409C Agents comprising midkine or its inhibitor as active ingredient Midkine (MK), which is a retinoic acid-inducible heparin-binding growth factor, enhances neutrophilic migration and exists in an inflammatory state at a high concentration. The midkine or its inhibitors can be used for treating neutrophilic functional disorders or inflammatory diseases.
CN101856489A Swine health granules and preparation process thereof The invention discloses swine health granules, which are granules prepared by using gentian, atraotydin, bupleurum, dried ginger, sodium bicarbonate, starch, sucrose powder as raw materials, wherein the granules comprise no less than 2.0 percent by weight of gentiopicrin, no less than 0.05 percent by weight of atractylenolide III and no less than 11.0 percent by weight of sodium bicarbonate. A preparation process of the swine health granules comprises the following step of: extracting gentian by using ethanol; carrying out steam distillation on atraotydin and bupleurum to extract essential oil of atraotydin and bupleurum; carrying out water extraction on dried ginger, sodium bicarbonate, gentian dregs obtained by ethanol extraction and atraotydin and bupleurum dregs obtained after the essential oil is extracted; mixing water extract with ethanol extract of gentian, which is obtained after ethanol is recovered, and aqueous solution obtained after atraotydin and bupleurum are distilled; after the mixture is subjected to ethanol precipitation treatment, concentrating the obtained product into a fluid extract; uniformly mixing the fluid extract with starch and sucrose powder and preparing granules from the mixture; and finally spraying the essential oil of atraotydin and bupleurum on the surfaces of the granules to obtain the swine health granules. The swine health granules of the invention represent an improvement of the preparation form of the conventional veterinary medicament, namely the swine health powder. The effect experiment shows that the curative effect of the swine health granules is obviously superior to that of the swine health powder.
US20050281910 Method for increasing pet activity A method for improving activity in a pet; especially elderly cats and dogs. The pets are administered a nutritional agent which promotes the growth of bifido- and lactic-bacteria in the gastrointestinal tract of a pet. The nutritional agent may be a prebiotic or a probiotic micro-organism, or both.
WO2012074856A3 Selective, lipophilic, and long-acting beta agonist monotherapeutic formulations and methods for the cosmetic treatment of adiposity and contour bulging Provided herein are pharmaceutical and cosmetic formulations and methods for regional adiposity reduction and treatment of body contour defects such as abdominal bulging; comprising an injectable formulation, said formulation comprising: an active ingredient that consists essentially of an adipose tissue-reducing amount of one or more lipophilic long-acting selective beta-2 adrenergic receptor agonists, or salts, solvates, or polymorphs thereof; and one or more subcutaneously acceptable inactive ingredients.
WO2006053166A1 8h-imidazo[4,5-d]thiazolo[4,5-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same The present invention provides for thiazolopyridine-based tricyclic compounds having the formula (I) wherein R1, R2, R5 and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
CN101028368A Medicinal use of radix rehmanniae polyose and its production An application of rehmannia polyose in preparing the medicines for preventing and treating the anaphylactia, such as allergic rhinitis, allergic asthma, allergic ophthalmopathy, allergic dermatopathy, atopic dermatitis and urticaria is disclosed.
CN102440999A Compound drug for preventing and curing iron-deficiency anemia and low anaphylaxis The invention relates to a compound drug for preventing and curing iron-deficiency anemia and low anaphylaxis, which mainly comprises the following components: 20% of iron-dextrin solution (computing by Fe), 2-5g of methylprednisolone sodium succinate, 20ml of propylene glycol and the like. The preparation has the greatest characteristics in that the iron-deficiency anemia can be prevented and cured, and simultaneously, the anaphylaxis of animals to the iron-deficiency anemia can be reduced, so that the stability of a product is improved.
CN103130781A Lincosamides antibacterial drug capable of being used for treating bacterial infection The invention relates to a lincosamides antibacterial drug capable of being used for treating a bacterial infection, and provides a lincosamides antibiotic of formula I or a pharmaceutically acceptable salt of the lincosamides antibiotic, wherein the lincosamides antibiotic can be used as an antibacterial agent. More specifically, a pharmaceutical composition containing compounds, a using method of the compounds and a preparation method of the compounds are provided. The compounds also have antibacterial activity to gram-negative bacteria, for example haemophilus influenza. Besides, compared with existing lincosamides antibacterial drugs, for example, clindamycin, the activity and the pharmacokinetic properties of the compounds are improved significantly.
EP1604970A1 2-(Biphenyl-3-yl)-carboxylic acids of gamma-secretase-modulating activity The present invention relates to compounds having the general formula (I) with the definitions of R1-R3 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds as a medicament, preferably for the treatment of Alzheimer's disease and their use for the modulation of g-secretase activity.
US20120114605 Methods and compositions relating to hematologic malignancies Methods of treating a subject having, or at risk of having, a myeloproliferative disorder are provided according to embodiments of the present invention which include administering a therapeutically effective amount of an arachidonate 5-lipoxygenase (5-LO) inhibitor to the subject. Combinations of therapeutic agents are administered according to embodiments of the present invention. In some embodiments, two or more 5-LO inhibitors are administered to a subject to treat a myeloproliferative disorder. In further embodiments, at least one 5-LO inhibitor and at least one additional therapeutic agent are administered to a subject to treat a myeloproliferative disorder. Methods of inhibiting leukemia stem cells are provided according to embodiments of the present invention which include contacting leukemia stem cells with an effective amount of an arachidonate 5-lipoxygenase inhibitor.
US20060116389 Antibacterial oxazolidinones A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: formula (I) wherein C is selected from D and E, formula (II) R2a, R6a, and R3a are independently selected from for example H, CF3, Me and Et; R2b and R6b are independently selected from for example H, F, CF3, Me and Et; R1b is —NRz-Z wherein Rz is for example hydrogen and Z is a 5- or 6-membered heteroaryl ring; R4 is for example an optionally substituted 5- or 6-membered heterocyclic ring system. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described.
US20100048547 Pi 3-kinase inhibitors and methods of their use Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases.
CN102341395A 3h-imidazo [4, 5 -c] pyridine- 6 -carboxamides as anti- inflammatory agents The present invention relates to compounds of general formula (I) in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.
CN101156857A A composite vitamine and its preparation method as well as application The invention relates to complex vitamin which comprises components of niacin, vitamin C, vitamin E, vitamin B 1, vitamin B 2, vitamin B 6 and vitamin A. The invention also provides a preparation method for the complex vitamin. The complex vitamin of the invention not only can be used for strengthening body resistance, but also be used for preventing or treating complex syndrome, facial acne, intractable tinea pedis and oral diseases, and the effect is obvious.
CN102000050A Nimesulide medicine composition for improving dissolution performance and preparation method thereof The invention provides a nimesulide medicine composition for improving dissolution performance and a preparation method thereof. The medicine composition in the invention comprises the following components in weight percentage: 1%-30% of nimesulide, 5%-30% of dispersing agent (at least one kind of liquid polyethylene glycol), 60%-85% of diluent (one or more of microcrystalline cellulose, lactose and starch), 1%-10% of silicon dioxide, 2%-20% of disintegrating agents (carboxymethyl starch sodium) and 0.1%-5.0% of adhesives (hydroxypropyl methylcellulose). The dissolution degree of the nimesulide medicine composition can reach above 90% within 5-10 minutes, and even 100%, thus the nimesulide medicine composition is different from the conventional solid composition of various medicines; and the nimesulide medicine composition improves the bioavailability of the nimesulide, is beneficial to clinical rapid fever abatement or pain killing and has high application value.
WO2008074445A1 Novel tricyclic and heterotricyclic derivatives, processes for preparing them, pharmaceutical compositions thereof The present invention concerns novel tricyclic and heterotricyclic derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
US20080039420 Method for inhibiting NOX1 gene expression The present invention relates to compositions and methods for gene-specific inhibition of gene expression by short interfering ribonucleic acid (siRNA) effector molecules. The compositions and methods are particularly useful in modulating gene expression of the NOX1 gene in colon cancer cells.
CN101849945A Voriconazole/clathrate stable compound pharmaceutical composition and preparation method thereof The invention belongs to the technical field of medicines, and discloses a voriconazole/clathrate stable compound pharmaceutical composition and a preparation method thereof. The composition comprises the following components in parts by weight: 1 part of voriconazole and 10-40 parts of clathrate stable compound. The composition has stable property, and is safe and effective for clinical use.
US20100056546 Sulfonylurea inhibitors of atp-sensitive potassium channels The present invention relates to new sulfonylurea inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.
WO2009008694A8 Pharmaceutical composition comprising the combination of an anti-depressive agent and an ansiolytic agent for control and treatment of depressive disorders The present invention concerns a pharmaceutical composition formed by the synergic combination of an anti-depressive selective 5-HT reuptake inhibitor, such as is the active principle: Sertraline and an ansiolytic agent belonging to the triazolobenzodiazepine group, such as is the active principle: Alprazolam, which are formulated in a single dosing unit to be administered by oral means in the form of capsules or tablets, the former being prescribed for the control and treatment of diseases such as: depressive disorders and related pathologies.
WO2013049272A3 Composition and method for treatment of symptoms associated with various skin conditions Compositions containing imidazole-based compounds, and optionally, colloidal oatmeal, for the treatment, prevention, and management of symptoms, conditions, diseases, and disorders of the skin. Also, methods for the treatment, prevention, and management of symptoms, conditions, diseases, and disorders of the skin using compositions containing imidazole-based compounds, and optionally, colloidal oatmeal.
CN101843618A Application of berberine and derivatives thereof in preparation of indole amine 2, 3-dioxygenase inhibitor The invention relates to novel application of berberine and derivatives thereof in preparation of medicines, in particular to application of berberine and derivatives thereof in preparation of indole amine 2, 3-dioxygenase IDO inhibitor, belonging to the medicine field. According to IDO inhibition activity detection, reversible inhibition judgment, inhibitor type judgment, Ki value determination and median effective inhibition concentration IC50 determination, the results show that berberine is reversible inhibitor and inhibition constant Ki is 8muM; and jatrorrhizine hydrochloride and palmatine hydrochloride are irreversible inhibitors, and the median effective inhibition concentrations IC50 thereof are respectively 123muM and 126muM. When the berberine and the derivatives thereof disclosed in the invention are used as IDO inhibitors, the application prospect is wide and the IDO inhibitors can be used for treating serious diseases such as cancers, AIDS, Alzheimer diseases, tristimania, cataract and the like with pathological feature of IDO-mediated tryptophan metabolism.
EP1322748B1 Stem cell differentiation-inducing promoter Provided is a stem-cell differentiation and induction promoter, which comprises as an effective ingredient a cyclohexenone long-chain alcoholic derivative represented by the formula (1):[wherein, R?1, R2 and R3¿ each independently represents a hydrogen atom or a methyl group and X represents a linear or branched C10-28 alkylene or alkenylene group]. Since the cyclohexenone long-chain alcoholic derivative according to the present invention promotes differentiation-induction of stem cells into cells expressing a specific biological function, a medicament comprising the derivative is useful as a preventive or remedial drug for diseases such as nervous diseases, bone diseases, circulatory diseases and myopathy, caused by the degeneration of tissues or cells or cell death.
US20110269691 Compositions and Methods for Treating Pigmentary Conditions and Melanoma A method of treating a hypopigmentary condition in a subject comprising administering to the subject an amount of SOX9 sufficient to treat melanoma is disclosed. The hypopigmentary condition can be a result of surgery, trauma or vitiligo. A method of treating a hyperpigmentary condition in a subject comprising administering to the subject an amount of inhibitor of SOX9 activity sufficient to treat melanoma is disclosed. A method of treating melanoma in a subject comprising administering to the subject an amount of SOX9 sufficient to treat melanoma is disclosed. A method of treating melanoma in a subject comprising increasing the amounts of retinoic acid and SOX9 in the subject by amounts sufficient to treat melanoma. A method of treating melanoma in a subject comprising administering to the subject an amount of prostaglandin D2 (PGD2) and retinoic acid (RA) sufficient to treat cancer. A method of sensitizing a melanoma cell to RA comprising administering to the subject an amount of SOX9 sufficient to decrease PRAME expression. A method of increasing p21 expression in a subject comprising administering to the subject an amount of SOX9 sufficient to increase p21 expression. Methods of screening for compounds that treat hypopigmentary conditions and/or melanoma are provided.
EP2613767A2 Compositions comprising a fatty acid oil mixture, a free fatty acid, and a statin Compositions comprising a fatty acid oil mixture, at least one free fatty acid, and at least one statin or pharmaceutically acceptable salt, hydrate, solvate, or complex thereof, and uses thereof are disclosed. Further disclosed are preconcentrates capable of forming a self-nanoemulsifying drug delivery system (SNEDDS), a self-microemulsifying drug delivery system (SMEDDS), or self- emulsifying drug delivery systems (SEDDS) in an aqueous solution.
CN1919189A Ibuprofen granule and preparing method thereof The invention relates to a novel ibuprofen granule and process for preparation, wherein the granule is prepared from 20 weight parts of ibuprofen and 80 weight parts of auxiliary materials, the auxiliary materials comprise the following constituents (by weight parts): starch gum 60-75 parts, hydroxyproxyl cellulose 2-10 parts, sodium cyclamate 1-7 parts. The process for preparing the granule comprises steps of disintegrating, sieving, making soft material, vacuum condensing and drying, finally granulating.
US20090143413 Thiazole Derivatives as CXCR3 Receptor Modulators The invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, which are antagonist of the CXCR3 chemokine receptor useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
CN102652745A Application of indole-3-carbinol (I3C) or dimer thereof to preparation of drugs for treating bone marrow suppression The invention discloses application of indole-3-carbinol (I3C) or a dimer 3,3'-diindolylmethane thereof to preparation of drugs for treating bone marrow suppression. I3C or the dimer thereof prevents white blood cell decrease while treating cancers and even increases the quantity of neutrophilic granulocytes, thus improving the chemotherapy effects of tumors, prolonging the lifetime of cancer patients and improving the quality of life.
CN103040750A Agomelatine liposome solid preparation The invention provides an agomelatine liposome solid preparation and a preparation method thereof. Agomelatine, di-stearoyl phosphatidyl ethanolamine and soyasterol are selected according to a specific weight ratio to be prepared into good-quality agomelatine liposome, and then the agomelatine liposome is prepared into the solid preparation with a general preparation method. The prepared agomelatine liposome solid preparation has the advantages of high entrapment efficiency, low leakage rate and uniform particle size, the stability and the reproducibility of the preparation are greatly increased, the drug release is delayed, the product quality and the bioavailability of the preparation are increased, the related substances are decreased, and the toxic and side effects are reduced.
US20100323988 Solid citrate and tartrate salts of dpp-iv inhibitors This invention relates to DPP-IV inhibitory citrate or tartrate salts of pyrrolidinylaminoacetyl pyrrolid acid compounds that are physically and chemically stable, substantially non-deliquescent solids under ambient conditions.
WO2008105325A1 Citrulline-containing beverage Disclosed is a beverage which can exert various useful functions of arginine, is easy to drink and has excellent stability. Specifically disclosed is a beverage containing 0.5 to 10% by weight of citrulline, 0.1 to 40% by weight of a sugar and 0.1 to 5% by weight of an organic acid.
US7521215 Polynucleotides, expression vectors, and host cells for culturing truncated tryptophanyl-tRNA synthetase polypeptides having chemokine activity; bioassay; drug screening; antitumor agents, antimetastasis agents Compositions comprising truncated tryptophanyl-tRNA synthetase polypeptides useful for regulating angiogenesis, as well as nucleic acids encoding such tRNA synthetase polypeptides are described. Methods of making and using such compositions are also disclosed.
CN1850813A Degradeable furan sesterterpenes keratinous spongistatin, and its preparing method and use This invention relates to degradation furan bi hemiterpene compound horny sponge lement separated getting from Sarcotragus sp animal. It is represented by formula (1). This invention also relates to its preparation method and its application in curing cancer, especially lung cancer, human uterus cancer, human central nervous system cancer, human skin cancer, human large intestine cancer. Middle cell toxity is contained in this compound, maximal restrain ratio to the cancers said above is normally more than or equal to positive medicine cisplatin and adriamyci, its IC50 value is around 10 mug/mL, so its good restrain function to cancer cell growth is displayed.
CN102727504A Application of salidroside in preparation of drugs for treating gastrointestinal barrier injury The invention discloses an application of salidroside in preparation of drugs for treating gastrointestinal barrier injury. Salidroside can improve intestinal nutrition, avoid gastrointestinal mucous membrane barrier function injury and resultant diseases, and substitute for existing intestinal nutrition preparations; and has the advantages of definite curative effect, rapid on-set, abundant resource, and low cost.
WO2013156659A1 Antitumour activity of taiwaniaquinoids and related compounds The invention relates to the use of a compound of general formula (I) for producing a drug for the treatment and/or prophylaxis of a solid cancer selected from breast cancer, colorectal cancer, lung cancer, pancreatic cancer, liver cancer and neuroblastoma, and for the treatment and/or prophylaxis of acute and chronic myeloproliferative syndromes.
EP2370426A1 N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and uses thereof This invention relates to N-{[(1R,4S,6R)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.
CN103316355A Pseudorabies live vaccine and preparation method thereof The invention relates to a freeze-drying protective additive which is composed of 1 to 2% of NZ-Amine AS, 0.1 to 0.2% of monosodium glutamate, 5 to 10% of saccharose, 1 to 2% of M199, 0.1 to 0.3% of trehalose, 8 to 15% of hydrolyzed gelatin, and the balance of water. The freeze-drying protective additive is used for preparing a freeze-dried pseudorabies vaccine. A heat-resisting protective agent can minimize the damage of various physical and chemical factors of a product to virus activity during sub-packaging and freezing-drying processes, greatly reduces the titer loss of the virus before and after freezing and drying and keeps the loss of being not greater than 0.2 titer. A heat-resisting protective agent live vaccine is high in degree of resistance to aging, the loss ratio of the virus kept for 10 days under a condition of 37 DEG C is not greater than 0.5 titer; the heat-resisting protective agent live vaccine can be stored for 24 months at 2 to 8 DEG C, the titer of the vaccine is reduced a little, so that the problem that the vaccine in general transporting and storing needs strict cold chain condition, which leads to energy waste and inconvenient storage, can be solved effectively.
WO2014003224A1 Compositions for whitening skin comprising madecassoside The present invention relates to a skin whitening composition comprising madecassoside as an active ingredient. The composition comprising madecassoside can be safely on the skin without causing side effects and has excellent effects of inhibiting the UV-induced production of skin darkening cytokine in keratinocytes and inhibiting the production of melanin in melanocytes to inhibit pigmentation. Thus, the composition comprising madecassoside as an active ingredient is very effective in inhibiting UV-induced pigmentation, inhibiting dark skin discoloration and whitening the skin.
US20120149731 New medical use The present invention relates to a method of treatment of urticaria comprising administration to a patient in need thereof an amount of the compound 3-(4-{[4-(4-{[3-(3,3-dimethyl-1-piperidinyl) propyl]oxy}phenyl)-1-piperidinyl]carbonyl}-1-naphthalenyl)propanoic acid, or a pharmaceutically acceptable salt thereof.
US20090215842 Method of Treating Schizophrenia Prodrome The present invention relates to a method of treating schizophrenia prodrome in human subjects using a NMDA glycine site agonist, a glycine transporter-1 inhibitor or mixtures thereof, optionally in combination with a pharmaceutically acceptable additive, carrier or excipient.
US20080262026 1-(2,4-dichlorophenyl)-2-{4-[(3,3-difluoropyrrolidin-1-yl)methyl]phenyl}-3-methyl-5-piperidin-1-yl-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one; obesity, psychiatric and neurological disorders Certain 4,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one and 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, methods for their therapeutic use and pharmaceutical compositions containing them are described.
US20100196509 Methods for Diagnosis and Treatment of Endometrial Cancer The present invention discloses methods of using endothelial membrane protein 2 (EMP2) as a biomarker for stratification of endometrial premalignancy, diagnosing, staging and imaging of endometrial neoplasia. Further, methods for identifying pharmaceutical/therapeutic modalities are described, including compositions which modulate glycolipid-enriched lipid raft microdomains (GEMs).
EP1307425B1 Novel n-(2-phenyl-3-aminopropyl)naphtamides A compound having general formula (I) and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
WO2007002272A1 Benzopyranone compounds for treating cancer This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound to a patient in need thereof. The Benzopyranone Compounds have the Formula (I) including pharmaceutically acceptable salts thereof, wherein R1 and n are as defined herein.
WO2008047658A1 Animal feed additive and animal feed An object is to provide a safe and convenient means for preventing or treating a disease in an avian or mammal, particularly a farm animal, specifically to provide a means for preventing or treating an inflammatory disease in a farm animal induced by a gram-negative bacterium. Another object is to improve the ruminal fermentation in a ruminant animal to contribute to the reduction in generation of heat-trapping gas and also improve the feed efficiency. Mannosylerythritol lipid (MEL) and/or rhamnolipid (RL) is fed to an avian or mammal.
US7763647 Topical solution containing a chromane or chromene derivative The invention relates to compositions intended for external topical use comprising a true solution containing a chromane or chromene derivative having formula (I), preferably a flavonoid, dissolved in a suitable solvent. The invention also relates to a method for preparing such compositions and the use of said compositions as sun protection agents for the skin, advantageously as agents having an anti-erythemal, anti-oxidant, anti-radical, anti-inflammatory or vasculotropic activity.
WO2014104929A1 Pharmaceutical composition for treatment of hiv infections The invention relates to the field of the chemical and pharmaceutical industry, and specifically to a pharmaceutical composition for treating HIV infections, containing as active ingredient at least one HIV protease inhibitor and also pharmaceutically acceptable auxiliary substances with a specific quantity ratio of components. In addition, the invention relates to a method for producing said composition and to a treatment method. The pharmaceutical composition according to the present invention has enhanced bioavailability and improved technological characteristics when compared to the prior art drug.
US7776861 Cycloheteroalkenyl compounds used as analgesics and for treating incontinence, inflammatory bowel disease, Parkinson's disease, amyotrophic lateral sclerosis, dementia, epilepsy, retinopathy, pruritus, psychoses, Huntington's disease, headaches, vomiting, dyskinesia or as anxiolytics and antidepressants A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.
US7968680 Polynucleotides encoding members of the human B lymphocyte activation antigen B7 family and polypeptides encoded thereby The present invention provides novel isolated BLAA polynucleotides and the membrane-associated or secreted polypeptides encoded by the BLAA polynucleotides. Also provided are the antibodies that immunospecifically bind to a BLAA polypeptide or any derivative, variant, mutant or fragment of the BLAA polypeptide, polynucleotide or antibody. The invention additionally provides methods in which the BLAA polypeptide, polynucleotide and antibody are utilized in the detection and treatment of a broad range of pathological states, as well as to other uses.
EP2136802A2 Use of fungicides for treating fish mycoses The invention relates to a method for protecting fish and invertebrates and all of the stages of development thereof from mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other significant species in aquaculture, using the above-mentioned selected fungicides, leading to an inihibition or destruction of pathogenic fungi. The means containing at least one fungicide selected from the above-mentioned group for use in fish-farming and fish-keeping is suitable for the prophylaxis and treatment of diseases affecting fish in aquaculture, farming ponds, farming tanks, aquariums, natural game fish waters, ponds and marine fish farms. The associated forms of application are addition to water and food and direct application. The addition of the inventive means to the water prevents spawn and fish from being infected by fungi.
US6894188 Adrenergic nblocking agent; benign prostatic hyperplasma The optically active compound, R(−)-5-[2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-2-hydroxybenzenesulfonamide in good optical purity, a metabolite of the α1-adrenergic blocking agent tamsulosin, and methods for the preparation thereof. Pharmaceutical compositions including the optically active compound and methods of treatment comprising administration of an effective α-adrenergic antagonistic amount of such compositions to mammals.
CN102379895A Compound for treating paratyphoid fever of cat and preparation method thereof The invention discloses a compound for treating paratyphoid fever of cat and a preparation method thereof, and aims to provide a compound for treating paratyphoid fever of cat and reduce probability of bacterial drug resistance occurrence and a preparation method thereof. The compound comprises the following components in percentage by weight: 2 to 10 percent of florfenicol, 1 to 5 percent of ofloxacin, 3 to 10 percent of taurine, 2 to 10 percent of sodium chloride, 2 to 10 percent of potassium chloride, 1 to 5 percent of vitamin K3, and the balance of glucosum anhydricum. In the compound, the florfenicol and the ofloxacin serving as antibacterial components can effectively kill salmonella, and is effective to escherichia coli and other bacteria, and combination of the florfenicol and the ofloxacin can reduce the probability of bacteria drug resistance, so that the effect of sterilization and bacteriostasis is reinforced; the taurine has the functions of resisting inflammation, protecting liver and abating fever, and an effect of symptomatic treatment to clinical symptoms caused by paratyphoid fever of cat; the sodium chloride and the potassium chloride can supply electrolyte; the vitamin K3 has an effect of stopping bleeding; and the drugs are combined to treat the paratyphoid fever of cat from various aspects, so that therapeutic errors are reduced.
US20080058381 Such as 1-[bis(4-chlorophenyl)methyl]-3-[(3,5-difluorophenyl)(methylsulfonyl)methylene]azetidine The present invention relates to the combination of a CB1 receptor antagonist and of sibutramine, to the pharmaceutical compositions comprising them and to their use in the treatment of obesity.
US20110166138 Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.
WO2008061429A1 Use of triacontanol in preparation of medicaments for treatment of cancers Use of triacontanol in preparation of human medicaments for treatment of cancers, especially liver cancer, intestinal cancer, and lung cancer. Triacontanol can be formulated into many formulations, such as oral tablets, capsules, drop pills, sustained-released formulations, injectable solution, injectable powder, suspension, and emulsion.
CN101040903A Farinfrared emplastrum The invention relates to an emplastrum for promoting blood circulation, repercussion and relieving pain, which includes lining cloth, gum base material and an anti-seizing layer, wherein the gum base material mainly comprises (by weight percent) rubber or propenoic acid pressure-sensitive adhesive 89-94, far infrared ceramic micro powder 3-6, peppermint oil 1-2, camphor oil or baras camphor 1-3.
EP2353592A1 Therapeutic causing contraction of mucosal tissue and method of treating diseases relating to mucosal tissues It is intended to provide a therapeutic causing contraction of a mucosal tissue whereby various diseases relating to mucosal tissues can be easily, safely and little invasively treated, a method of treating various diseases relating to mucosal tissues with the use of the therapeutic causing contraction of a mucosal tissue. Namely, a therapeutic causing contraction of oral pharyngeal mucosal tissue containing ethanol as the active ingredient together with a steroid.
CN1907292A Emulsion of baicalin for injection and its preparation process The invention relates to an emulsion for injection and preparing process, wherein each 1000ml of the injection comprises the following constituents (by weight parts): baikal skullcap root glycosides 1.0-200.0g, vegetable oil for injection 50-300g, emulsifying agent 5-20g, isotonic conditioning agent 20-60g, and balancing water.
US20050147666 Rapidly disintegrates in the oral cavity without water and has a practical hardness; comprises a water soluble active ingredient, D-mannitol in the form of crystals or fine particles and crospovidone According to the present invention, provided are an intraorally rapidly disintegrable tablet which comprises D-mannitol and a disintegrator in addition to fine granules prepared by granulating a mixture of a water-soluble pharmacologically active ingredient and an adsorbent; a process for producing an intraorally rapidly disintegrable tablet which comprises mixing D-mannitol and a disintegrator with fine granules prepared by granulating a mixture of a water-soluble pharmacologically active ingredient and an adsorbent to yield a material for compression molding, and subjecting the material to compression molding; and an intraorally rapidly disintegrable tablet which is prepared by mixing D-mannitol and a disintegrator with fine granules prepared by granulating a mixture of a water-soluble pharmacologically active ingredient and an adsorbent to yield a material for compression molding, subjecting the material to compression molding.
CN103652924A Compound grape seed oil soft capsule and preparation method for compound grape seed oil soft capsule The invention belongs to the technical field of microemulsion formulas for grape seed oil, and discloses a compound grape seed oil soft capsule and a preparation method for the compound grape seed oil soft capsule. The compound grape seed oil soft capsule includes contents and a capsule shell, wherein the contents are prepared from following raw materials: grape seed oil, procyanidine, licoisoflavone, and a W/O (water-in-oil) emulsifier; the capsule shell is prepared from raw materials including gelatin, glycerinum, glucomannan and water, and the weight ratio of the gelatin to the glycerinum to the glucomannan to the water is 100 to (45-55) to (0.1-0.2) to 70. The compound grape seed oil soft capsule provided by invention adopts the microemulsion technique, so as to effectively solve the problem of miscibility and achieve the synergy function; the soft capsule achieves higher stability, is low in cost, and is quickly disintegrated in a human body and easily absorbed, so as to perform the synergic healthcare function; the invention has the advantages of reasonable formulation, advanced technique, simple equipment, small investment, and remarkable social and economic benefits.
US20090192099 Prodrugs of heteroaryl compounds The present invention provides hydrophobic prodrugs of bases, nucleosides, and nucleotides as well as methods of using the prodrugs as antiviral and anti-cancer chemotherapeutic agents.
US6974819 Alzheimer's disease; Parkinson's disease; Pick's disease; bipolar disorders; schizophrenia; alopecia; anticancer agents Imidazo[1,2-α]pyrimidinones and pyrimido[1,2-α]pyrimidinones useful for preventive and/or therapeutic treatment of neurodegenerative diseases, such as Alzheimer's disease, caused by abnormal GSK3β activity.
CN102643256A Arylglucoside compound and preparation method and application thereof The invention discloses an arylglucoside compound which is shown as a formula I or a formula I', pharmaceutically acceptable salts of the arylglucoside compound, optical isomers of the arylglucoside compound or prodrugs of the arylglucoside compound. The invention additionally relates to a preparation method and application of the arylglucoside compound. The arylglucoside compound provided by the invention has a very good inhibitory activity to sodium-glucose co-transporters (SGLT), especially SGLT2, and is an antidiabetic drug with a very great potential.
EP1597240B1 Bicyclic heterocycles, medicaments containing said compounds, use thereof, and method for the production thereof The invention relates to bicyclic heterocycles of general formula (I), wherein Ra, Rb, Rc, Rd, Re, and X have the definitions indicated in claim 1, the tautomers, stereoisomers, mixtures, and salts thereof, especially the physiologically acceptable salts thereof containing inorganic or organic acids having valuable pharmaceutical properties, especially an inhibiting effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, especially cancer diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the production thereof.
CN101712710A LMP1targeted oligonucleotide and application thereof serving as radiotherapeutic sensitizer The invention relates to an EBV virus LMP1 targeted oligonucleotide and also relates to application of the oligonucleotide in treatment and radiotherapeutic sensitization of nasopharyngeal darcinoma. The oligonucleotide has the following characteristics that: (1) the oligonucleotide is complementary with an EBV LMP1 gene through the oligonucleotide binding sequence; (2) the oligonucleotide consists of 11-70 ribonucleotides, and the ribonucleotides are connected by organic phosphate bonds from the 5' direction to the 3' direction; (3) the 2' site of ribose has a methoxy-substituted radical; and (4) the 3' end is connected with a butanol radical. The modified oligonucleotides have relatively high enzymolysis resistance and biological activity, and can serve as an effective medicine for treating or assisting to treat nasopharyngeal darcinoma or EBV relevant diseases.
WO2010020703A1 Mek 1/2 inhibitors for the treatment of peritoneal fibrosis Drugs useful in the prevention and treatment of fibrosis of the peritoneal membrane (peritoneal opacification, tanned peritoneum syndrome, mural fibrosis and sclerosing peritonitis syndrome), which arises as a consequence of long-term peritoneal dialysis, method for selecting such drugs and method for collecting data that are useful in the diagnosis of said disease.
US20110212080 Urea derivatives as antibacterial agents This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
US8138170 Inhibiting transplant rejection and inflammatory cell accumulation; wound healing agents, antiallergens The present invention provides compositions and methods comprising ningalins for use in modulating immune responses to infection, injury, allergy and/or transplantation.
US20100004179 Targeting of ews-fli1 as anti-tumor therapy Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.
US20130210898 Recombinant viruses and their use for treatment of atherosclerosis and other forms of coronary artery disease and method, reagent, and kit for evaluating susceptibility to same Recombinant viruses comprising a heterologous. DNA sequence coding for a lipase involved in lipoprotein metabolism. The invention also concerns the preparation and use in therapy of said recombinant viruses, especially for the treatment or prevention of dyslipoproteinemia-related pathologies.
US7939639 Functional role of adrenomedullin (AM) and the gene related product (PAMP) in human pathology and physiology The methods of the present invention demonstrate that adrenomedullin (AM) is expressed in human cancer cell lines of diverse origin and functions as a universal autocrine growth factor driving neoplastic proliferation. The present invention provides for AM peptides and AM antibodies useful in therapeutic, pharmacologic and physiologic compositions. The present invention additionally provides for methods of diagnosis, treatment and prevention of disease utilizing compositions comprising the AM peptides and antibodies of the present invention. The methods of the present invention also provide for experimental models for use in identifying the role of AM in pancreatic physiology. The methods pertaining to rat isolated islets have show that AM inhibits insulin secretion in a dose-dependent manner. The monoclonal antibody MoAb-G6, which neutralizes AM bioactivity, was show by the methods of the present invention to increase insulin release fivefold, an effect that was reversed by the addition of synthetic AM.
EP1682540A1 Azolidinecarbonitriles and their use as dpp-iv inhibitors The invention discloses a novel heterocyclic compounds that falls within f the ambit of general formula (I), its stereoisomers, pharmaceutically acceptable salts or solvates wherein X, n,k,z, R1, R2, R3, R4, R5 and R6 are as defined in the specification that are useful in (i) normalizing elevated blood pglucose levels in diabetes, (ii) treating disorders related to glucose intolerance and (iii) for scavenging free radicals of mammals. The invention also discloses pharmaceutically acceptable composition comprising these compounds, method for preparation of the compounds as defined bove and method of treating mammals including human beings by administering an effective amount of said compounds to a subject in need thereof. The invention further discloses use of these compounds in the manufacture of a medicament useful for treatment of different disease conditions as stated above.
US7115602 Antiinflammatory agents; respiratory system disorders; autoimmune disease The invention relates to 7-(4-tert butyl-cyclohexyl)-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
EP2742974A1 Phenanthrene derivatives for use as medicaments Phenanthrene derivatives of formula I for use as medicaments. The present invention refers to phenanthrene derivatives for use as medicaments, mainly in the prevention and/or treatment of DM1, HDL2, SCA8, DM2, SCA3, FXTAS, FTD/ALS, and SCA31. In a preferred embodiment, phenanthrene derivatives of the invention are also used as antimyotonic agents.
CN101889988A Tiamulin fumarate effervescent granules for treating pneumonia and dysentery of livestock and poultry The invention relates to tiamulin fumarate effervescent granules for treating pneumonia and dysentery of livestock and poultry, which comprise the following raw materials and auxiliary materials in part by weight: 80 to 120 parts of tiamulin fumarate, 100 to 140 parts of citric acid, 150 to 170 parts of sodium bicarbonate, 20 to 40 parts of polyethylene glycol 6000, 190 to 230 parts of dextrin and 360 to 400 parts of sucrose. A method for preparing the tiamulin fumarate effervescent granules comprises the following steps of: grinding the raw materials and the auxiliary materials, respectively mixing the ground raw materials and the ground auxiliary materials, drying the mixture, pelletizing the dried mixture and sufficiently mixing the products. The tiamulin fumarate effervescent granules prepared by the method are used for diseased livestock and poultry in an oral administration mode, have the advantages of good taste and stable quality and are an ideal preparation for treating mycoplasma pneumonia, actinomycotic pleuropneumonia and treponema dysentery of the livestock and poultry currently.
EP1137414B1 Use of acetylcholinesterase inhibitors on the modulation of the hypothalamic-pituitary-gonadal axis Acetylcholinesterase inhibitors are of use for treating a variety of conditions that can benefit from stimulation of the hypothalamic-pituitary-gonadal axis such as failure of ovulation, some cases of unexplained infertility, luteal phase defect, hypogonadotrophic hypogonadism, aesthenozoospermia, oligozoospermia, delayed onset of puberty and crytorchidism. Suitable acetylcholinesterase inhibitors include donepizil, rivastigmine galanthamine, lycoramine and analogs thereof.
WO2006099884A1 Beta-aminoalcohol antibiotics This invention concerns antimicrobially active compounds of the formula (I) wherein R1 represents alkyl, alkoxy, halogen or cyano; R2 represents hydrogen or halogen; R3 represents hydrogen or halogen; one of the symbols W1 and W2 represents CH and the other represents CH or N; U represents oxygen or sulphur; and V represents CO or CH2; as well as their optically pure enantiomers, mixtures of enantiomers, racemates, optically pure diastereoisomers, mixtures of diastereoisomers, diastereoisomeric racemates, mixture of diastereoisomeric racemates, meso forms, pharmaceutically acceptable acid addition salts, solvent complexes and morphological forms thereof.
WO2010070672A3 Phytochemical composition comprising cafeic acid derivatives The present invention is successful in providing caffeic acid derivatives namely eicosanyl caffeate and docosyl caffeate from Glycyrrhiza. Also, the present invention provides a composition comprising said bio actives and also provides a process to prepare the composition. Ultimately, the invention provides solution for the management of ulcer.
US20130053425 Method for Lowering Intraocular Pressure Using Gap Junction Blockers A pharmaceutical composition contains a gap junction blocker, and a pharmaceutically acceptable carrier. In addition, a pharmaceutical composition contains a gap junction blocker, a pharmaceutically acceptable carrier, a preservative and a buffer. Also, a method of lowering intraocular pressure includes the step of administrating to a subject a pharmaceutical composition containing a gap junction blocker, and a pharmaceutically acceptable carrier.
WO2006098314A1 Novel sugar uptake activator and method for screening the same A sugar uptake activator containing a substance having a PGC-1β action as an active ingredient and a method for screening a sugar uptake activator comprising the steps of bringing a test substance into contact with a PGC-1β gene promoter and analyzing the activity of the PGC-1β gene promoter are disclosed. The sugar uptake activator is a novel therapeutic agent for diabetes that facilitates sugar uptake in a muscular tissue in a hyperglycemic condition regardless of blood insulin level.
CN103083356A Anti-allergic and anti-inflammation water The invention discloses anti-allergic and anti-inflammation water special for resisting allergy of human skin under external stimulation. The anti-allergic and anti-inflammation water is prepared from 0.6 to 2.0 parts of boric acid, 0.02 to 0.06 part of chlorhexidine acetate, 0.4 to 0.8 part of dipotassium glycyrrhizate, 6 to 10 parts of glycerol and 93 to 86 parts of distilled water through mixing, heating, heat preservation and cooling. The anti-allergic and anti-inflammation water has the following advantages that 1, quick response: because the product can be sprayed or applied to the surface of the allergic skin, the effect is achieved in a few minutes; 2, comprehensive functions: the product has anti-inflammation, sterilization and cleaning functions besides an anti-allergic function, so the product can comprehensively treat the affected part; and 3, low cost: the cost of each kilogram of the product does not exceed *yuan through rough calculation, so the product is popular with vast patients.
EP2765992A1 Foam formulations The present invention provides foamable pharmaceutical compositions comprising water-soluble antibiotics and anti-inflammatory steroids and methods of preparing same. Particularly, the present invention relates to oil-free pharmaceutical compositions comprising a quinolone, an anti-inflammatory steroid, a polar co-solvent, and propellant gas, administered to the ear in the form of foam for treating ear disorders.
CN101007040B External applied medicine for treating bone fractures The invention discloses an externally-used medicament for treating bone fracture, which is prepared from the raw materials of drynaria, native copper, wood louse, leopard bone, hairy deerhorn, safflower, cortex acanthopanacis, dipsacus root, frankincense, myrrh and musk through grinding into micro-powders.
CN102188416A Medicine controlling and curing chronic aplastic anemia Provided is a medicine controlling and curing chronic aplastic anemia. The medicine is composed of a mixture comprising, by weight percentage, 12 to 32 percent of hexadecanoic acid , 9.0 to 34 percent of hexadecylenic acid, 15.3 to 32 percent of 9-octadecenoic acid, 0.3 to 4.6 percent of stearic acid, 10.8 to 26 percent of 9, 12-octadecadienoic acid and 3.6 to 36 percent of 9,12,15- octadecatrienoic acid. Compared to other medicines, the medicine has simple components and possesses effects of activating marrow hematopoiesis, promoting marrow cell fifferentiation and being a target organ stimulant. The medicine can achieve the effect of adjusting and improving hematopoiesis microenvironment and helping a body perform multi-way signal transduction. The medicine is characterized by good curative effect, safety and simplicity.
US20070259866 Method of Adenovirus, HIV and HPV Prophylaxis The likelihood of infection by a broad spectrum of viruses, including Adenovirus, Human Immunodeficiency Virus and/or Human Papillomavirus infection can be reduced by the prophylactic topical application, prior to the exposure to or infection by the virus of metallo-organic cobalt compounds according to the following formula to the site of infection: wherein each A may be the same or different and is an alkyl group, a phenyl group or a substituted derivative of a phenyl group; wherein each Y may be the same or different and is hydrogen, an unbranched alkyl group, a halide or a group having the structure wherein R is hydrogen, an alkoxide group, and alkyl group, or OH; wherein each B may be the same or different and each is hydrogen or an alkyl group; wherein each X may be the same or different and each is a water soluble group having weak to intermediate ligand field strength; and Z− is a soluble, pharmaceutically acceptable negative ion. Metallo-organic cobalt compounds may also be used to disinfect liquids which contain adenovirus, Human Immunodeficiency Virus and/or Human Papillomavirus.
US20120232126 Multi-targets interfering rna molecules and their applications This invention relates to interfering RNA (iRNA) molecules and their applications, especially multi-targets iRNA molecules and their applications. The said multi-targets iRNA molecules comprised of a sense strand annealed onto at least one antisense strand, each strand is at least 30 nucleotides in length, the sense or antisense strand has at least two segments, which can target at least two RNAs of different genes, or can target at least two portions of an RNA, and wherein the iRNA does not induce an interferon-response when transfected into a cell. The iRNA molecule can interfere with the translation procedure post-transcription, and the target gene is inhibited or blocked, the iRNA does not induce an interferon-response in vivo. The RNA molecules are the active ingredient in preparation of the drug which can regulate one or many genes function.
CN102905763A Lipids, lipid compositions, and methods of using them Disclosed are formulation and optimization protocols for delivery of therapeutically effective amounts of biologically active agents to liver, tumors, and/or other cells or tissues. Also provided are compositions and uses for cationic lipid compounds of formula (I). The invention also relates to compositions and uses for stealth lipids of formula (Xl). Also provided are processes for making such compounds, compositions, and formulations, plus methods and uses of such compounds, compositions, and formulations to deliver biologically active agents to cells and/or tissues.
US20080312237 Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
US20100280033 Pyrazole Derivatives The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrazole compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.
CN102232948A Application of diterpene lactone compound or plant extract thereof and medicinal composition The invention discloses application of a diterpene lactone compound or plant extract thereof shown in the formula I to preparation of an activation inhibitor for herpes simplex virus, application to preparation of a medicament for resisting symptoms caused by the herpes simplex virus as well as a medicinal composition containing the diterpene lactone compound or plant extract thereof shown in the formula I. According to the invention, the inhibitory activity of the iterpene lactone compound or plant extract thereof shown in the formula I to the herpes simplex virus (HSV) is found, thereby a new medical application field is opened for the diterpene lactone compound or plant extract thereof and a new path is provided for preventing and treating the symptoms caused by the herpes simplex virus.
CN1827590A Novel pregabalin crystalline form, its preparing process and pharmaceutical compositions thereof The invention relates to a new crystal system, a method for preparation of pregabalin which can be used as medicines for curing epilepsy and peripheral neuralgia and its medicinal compounds. The crystalline pregabalin has many advantages. For example, its stability is good, it is suitable for mass production, its quality can be controlled and so on.
US20090131420 Novel Heterocyclic Analogs of Biphenyl Ethers The present invention relates to novel compounds of formula (I) and their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic analogs of biphenyl ethers of the general formula (I).
CN102579665A Medicinal golden cypress paste for treating stubborn psoriasis and preparation method The invention relates to a medicinal golden cypress paste for treating stubborn psoriasis and a preparation method. The preparation method comprises the following steps of: grinding orpiment, calomel, indigo naturalis, mirabilite into fine powder; putting rheum officinale, coptis chinensis, radix paeoniae rubra and the like in a boiler for boiling after immersing them by using clear water; filtering and removing dregs, and concentrating by slow fire till a thick paste state is formed; and mixing the thick paste with the fine powders, such as orpiment, calomel, adding white wine, and stirring the mixture till the mixture is in paste state. The medicinal golden cypress paste has the advantages of strong killing effect on dermatophytes, particularly remarkable effect for treating psoriasis and capability of being applied to the treatment of other dermatophytosis.
CN102753188A Methods for treating brain tumors The present invention relates to methods treating brain tumors comprising administering a subject in need thereof a therapeutically effective amount of sodium meta arsenite, alone or in combination with another anti-brain tumor medicament.
CN102872260A Method for treating and/or preventing inflammation and cutaneous photodamage by using water soluble extract from plant of Solanum genus and having photoprotective effect The invention provides a method for treating and/or preventing inflammation and cutaneous photodamage by using a water soluble extract from the plant of Solanum genus and having a photoprotective effect. The water-soluble extract of the nightshade contains solasonine and solamargine.
US20110178176 Use of a virucidal preparation on an area of the face for prevention of transmission or contraction of viral illnesses, or to shorten the duration of, or lessen the severity of viral illnesses A method of reducing or inhibiting the contraction or communication of viral illnesses is proposed. Application of a virucidal preparation containing one or more organic acids (e.g. malic acid) with or without a surfactant (e.g. sodium C14-C16 olefin sulfonate) in a carrier agent (e.g. petrolatum) to the face of well individuals will reduce the chance that they contract illness with viral illnesses such as viral upper respiratory illnesses, influenza, viral gastroenteritis, viral rhinosinusitis, viral cold sores, and viral conjunctivitis. Application of said ointment to the nares of individuals with a VURI will reduce the chance they transmit the illness by reducing self-contamination of their hands when touching their nose. In addition, individuals suffering from a cold or influenza may reduce the duration or severity of illness by application of the nasal antiviral ointment. The ointment is most effective when applied with a clean applicator two or three times daily.
CA2567621A1 Herbal product comprising cinnamon, bitter melon and omega-3 fatty acids This invention relates to a new herbal product comprising cinnamon (Cinnamomi cassiae: Cinnamonum verum) and bitter melon (Momordica charantia) and omega-3 fatty acids and, optionally, chocolate. Each of these ingredients is known to demonstrate therapeutic effects but the combination of the three ingredients demonstrates significant synergism and improved therapeutic effects.
CN101239958A Arylthioureas compounds with antivirus activity, preparation method and use thereof The invention relates to arylthiourea compounds, a preparing method and application thereof. The invention provides compounds of formula (I), wherein, R1, R2, R3, R4 represent one or more groups of hydrogen, alkyl, halogen and alkoxy, the groups represented by R1, R2, R3, R4 can be same or not. The invention also provides methods for preparing the compounds. The compounds has excellent effect of restraining HIV virus.
CN102552289A Composition for treating diabetes and preparation method The invention relates to a Glipizide composition for treating diabetes, which is characterized in that unit dosage of composition contains 2.5-5mg of Glipizide, 45-50mg of starch, 23-28mg of dextrin, 0.8-1.3mg of silicon dioxide, 0.20-0.40mg of magnesium stearate, and 20-28mg of sucrose. According to the invention, the dissolution rate of the Glipizide composition is improved and the related substance content in the composition is reduced.
CN102600379A Unique prescription for treating severe cough and asthma The invention falls into high technology and medical field, and aims to rapidly treat severe cough and asthma due to intoxication of respiratory tract. The technical scheme includes (1) administering Herba Lobeliae Chinensis, Herba Polycarpaeae Corymbosae, Radix Notoginseng and fruit of Yucca Gloriosa L. directly or after soaking in wine, to relieve inflammation and inhibit bacteria; (2) drinking dews on grapefruit tree and bamboo leaves to moisturize lung; (3) administering uncooked peanut and lean meat rib radish soup to activate and nourish blood; (4) performing moxibustion with mulberry to clear away toxic substances; (5) utilizing HUASHENGLONG to clear away toxic substances and strengthen physical fitness; and (6) administering flower/fruit of Rohdea Japonica Roth. and snow to treat cough and asthma. The prescription can heal cough and asthma.
US20070122351 Inhalation Drug Combinations A method for treating respiratory disorders by administrating by inhalation an effective amount of a β2-receptor agonist, an acceptable amount of a corticosteriod, and HFA 134a, to a patient in need thereof, is disclosed. Preferably, the β2-receptor agonist is salmeterol or a physiologically acceptable salt thereof, and the corticosteriod is fluticasone propionate or a solvate thereof. The combination of salmeterol, fluticasone proprionate, and HFA 134a may lower the risk of cardiac arrhythmias, sudden death, or hypercorticism that are sometimes associated with the simultaneous administration of a β2-receptor agonist and an anti-inflammatory corticosteroid.
CN103159736A Substitutional pyrazol kinase inhibitor The invention belongs to the field of medical technology, in particular to a substitutional pyrazol kinase inhibitor which is shown by general formulas (I), (II), (III) or (IV), salt or a stereoisomer which are acceptable in pharmacy, wherein R1, R2, L1and L2 are defined as same as the definitions in an instruction book. The invention further relates to preparation methods of the compounds, application of the compounds, the salt or the stereoisomer which is acceptable in pharmacy in the drugs of preparing, treating and/or preventing diseases which are related to or not related to cancers caused by mutation of b-RAF.
US20090170825 Beta-lactamylalkanoic acids for treating premenstrual disorders 0-lactamyl alkanoic acids are described. Methods for treating various premenstrual disorders using or more O-lactamyl alkanoic acids are also described.
WO2007064010A1 Preventive/therapeutic agent for alzheimer's dementia It is intended to provide a preventive/therapeutic agent for Alzheimer's dementia, characterized in that a ω-3 polyunsaturated fatty acid and thyroid hormone are used in combination. The preventive/therapeutic agent can be an alternative to a therapeutic method currently performed for Alzheimer's dementia or can achieve a high therapeutic effect by using the therapeutic method in combination and is excellent in safety.
CN101780088A Compound Ceftiofur Hydrochloride injecta The invention relates to compound Ceftiofur Hydrochloride injecta, which effectively solves the problems of local pain and the like caused by uneven content distribution, poor stability, large viscosity. The technical scheme adopted by the invention is as follows: the injecta is prepared from the following components by weight percent: 1-15% of Ceftiofur Hydrochloride, 0.5-7.5% of Sulbactam Sodium, 48-93% of polyethylene glycol and 5-50% of absolute ethyl alcohol, wherein the total amount is 100%; firstly the polyethylene glycol and the Ceftiofur Hydrochloride are mixed, stirred and dissolved, the absolute ethyl alcohol is added and evenly stirred, and the Sulbactam Sodium is added, stirred and dissolved; and a microfiltration membrane is used to filter under the temperature of 30-45 DEG C, the filtrate is subpackged in bottles, and the bottles are gladded, sealed and packed to obtain the injecta of the invention. The invention overcomes the defects of easy delamination and inconvenient use of Ceftiofur suspension injecta in the market, and provides the injecta with stability, even content and rapid absorption; and the compound Ceftiofur Hydrochloride injecta also can effectively cure bacterial infection producing extended-spectrum beta-lactamase (ESBL).
EP2453893A1 Treatment of non-neuronal and non-myocardial cell, tissue and organ damage and associated pain with persistent sodium current blockers The present invention relates to a method for slowing the development of mammalian organ, tissue and cellular damage and death by using a persistent sodium current blocker (or a pharmaceutically acceptable salt or derivative thereof). The present invention further relates to a method for preventing damage and death in mammalian organs, tissues and cells or reducing the extent of damage and death in mammalian organs, tissues and cells. In particular the invention relates to a method for the treatment, amelioration or prevention of non-neuronal and non-myocardial cell or tissue damage or death and for reducing the pain associated with non-neuronal and non-myocardial cell or tissue damage.
CN103040758A Drug composition containing cefathiamidine compound and preparation method of drug composition The invention provides a drug composition containing a cefathiamidine compound, which mainly comprises cefathiamidine, mannitol and sodium carbonate. The invention further provides a preparation method of the drug composition, which comprises the steps of weighing cefathiamidine, mannitol and sodium carbonate, drying and conducting air jet pulverization, screening powder with the particle size of 48-64 micrometers with a sieve, feeding cefathiamidine, mannitol and sodium carbonate to a mixer at a constant speed in proportion, stirring, sufficiently mixing, packaging, charging sterile nitrogen and conducting plug pressing and cover rolling. The drug composition has good stability, and is easy to store, good in solubility and convenient to use.
WO2007112648A1 The medicinal compositions comprising triptolide derivatives and its dosage form and application The present invention provides a medicinal composition, its application and dosage form. The composition comprises effective dosage triptolide derivatives of general formula (I), their optical isomers or their pharmaceutical acceptable salts, and conventional pharmaceutical adjuvant. The high efficient and harmfulless triptolide derivatives selected by the present invention can be used to treat tumor diseases. The medicinal composition of present invention can be prepared to the preparation suitable for absorption and utilization by tissue and organ of warm-hearted animals.
WO2008107334A2 Process for the synthesis of glyt-1 inhibitors Process for preparation of a compound of formula (I) wherein Het is a 6-membered heteroaryl group, containing one, two or three nitrogen atoms; R1 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl, NR4R5 or (C1-C6)-alkyl subtituted by halogen; R2 is hydroxy, halogen, NO2, CN, (C1-C6)-alkyl, (C3-C6)-cycloalkyl, (C1-C6)-alkyl substituted by halogen, (C1-C6)-alkyl substituted by hydroxy, (CH2)o-(C1-C6)-alkoxy, (C1-C6)-alkoxy substituted by halogen, NR4R5, C(O)R6 or SO2 R7; R3 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl or (C1-C6)-alkyl subtituted by halogen; R4 and R5 independently from each other are hydrogen or (C1-C6)-alkyl; R6 is hydrogen, (C1-C6)-alkyl, (C1-C6)-alkoxy or NR4R5; R7 is (C1-C6)-alkyl, (C1-C6)-alkyl optionally subtituted by halogen, (CH2)o-(C3-C6)-cycloalkyl, (CH2)o-(C3-C6)-alkoxy or NR4R5; n is 0, 1, 2 or 3; o is 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof, characterized in that it comprises the steps of a) reacting a compound of formula (21) with a compound of formula: R3 OH 8 to a compound of formula (11) and b) coupling the compound of formula (11) in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula (15) to obtain a compound of formula (I).
WO2014096133A1 Use of 3-carboxy-n-ethyl-n,n-dimethylpropan-1-aminium or a pharmaceutically acceptable salt thereof in the treatment of atherosclerosis Use of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium and its pharmaceutically acceptable salts: 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium hydrogen fumarate and 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium dihydrogen phosphate, in the prevention and treatment atherosclerosis.
US20110130459 Composition for accelerated production of collagen Here the inventors provide a composition for topical application to the skin of animal comprising stearidonic acid in combination with one or octadecatrienoic acids (CODTAs). Preferably the composition comprises echium oil as a source of the stearidonic acid, and a plant lipid as a source of octadecatrienoic acid, such as borage oil (Borago officinalis), wheat germ oil (Triticum vulgare) rosehip oil (refined; Rosa mosqueta), jacaranda oil (Jacandra mimosi folia), and/or calendula oil (Calendula officinalis). The composition of the invention increases collagen I secretion and thus has particular utility for promoting collagen production in skin.
WO2014001247A1 N-[4-(Quinolin-4-yloxy)cyclohexyl(methyl)](hetero)arylcarboxamides as androgen receptor antagonists, production and use thereof as medicinal products The invention relates to N-[4-(quinolin-4-yloxy)cyclohexyl(methyl)](hetero)arylcarboxamides, intermediates and methods for their production, use thereof for treating and/or preventing diseases and use thereof for producing medicinal products and use thereof for treating and/or preventing diseases, especially of hyperproliferative diseases.
US7109331 Antiprotozoa agents; 4-pyrrolidine pyrrolo(3,2-d)pyrimidine and 4-pyrrolidine pyrazolo(4,3-d)pyrimidine derivatives The present invention provides a compound of the formula (I): wherein A is selected from N, CH and CR, where R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH2, NHR1, NR1R2 and SR3, where R1, R2 and R3 are each optionally substituted alkyl, aralkyl or aryl groups; B is selected from OH, NH2, NHR4, H and halogen, where R4 is an optionally substituted alkyl, aralkyl or aryl group; D is selected from OH, NH2, NHR5, H, halogen and SCH3, where R5 is an optionally substituted alkyl, aralkyl or aryl group; X and Y are independendy selected from H, OH and halogen, with the proviso that when one of X and Y is hydroxy or halogen, the other is hydrogen; Z is OH, or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ and OQ, where Q is an optionally substituted alkyl, aralkyl or aryl group; and W is OH or H, with the proviso that when W is OH, then A is CR where R is as defined above; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof. The invention also provides pharmaceutical compositions comprising compounds of formula (I), methods of preparing compounds of formula (I), and methods of treatment using compounds of formula (I).
USRE41920 Isobutylgaba and its derivatives for the treatment of pain The instant invention is a method of using certain analogs of glutamic acid and gamma-aminobutyric acid in pain therapy.
CN102048721A Injection preparation The invention relates to an injection preparation and application thereof. The injection preparation is prepared by using an ibuprofen amino acid salt as a medical active component and combining with pharmaceutically acceptable excipients through a certain preparation process can be used for treating various types of pains and fever. Various injectable preparations such as a small-capacity injection, lyophilized powder, sterile powder, a large-capacity injection and the like are developed and prepared according to the technical scheme provided by the invention.
CN102552302A Compound josamycin nano-emulsion antibacterial drug and preparation method thereof The invention discloses a compound josamycin nano-emulsion antibacterial drug and a preparation method of the drug. The components of the compound josamycin nano-emulsion comprise josamycin, trimethoprim, glacial acetic acid, a surfactant, a cosurfactant, oil and distilled water; the particle size of the drug is 1nm-100nm, and the drug takes on light yellow or colorless clear transparent liquid and has the advantages of being high in bioavailability, small in toxic and side effects, low in viscosity, good in mobility, good in dispersibility, quick in absorption, stable in property and the like. The drug is mainly used for treating diseases caused by staphylococcus, streptococcus, pneumococcus, diplococcus meningitides and bordetella pertussis, clostridium difficile, corynebacterium diphtheria, bacillus anthracis, brucella, legionella, helicobacter, mycoplasma, rickettsia, chlamydia and the like.
EP1988889A2 Compositions and methods for treatment of ophthalmic diseases and disorders Provided herein are compositions and methods for treating ophthalmic diseases and disorders. Compositions comprising retinylamine derivative compounds provided herein are useful for treating and preventing ophthalmic diseases and disorders, including diabetic retinopathy diabetic maculopathy, diabetic macular edema, retinal ischemia, ischemia-reperfusion related retinal injury, and metabolic optic neuropathy.
EP1399406B1 Novel estrogen receptor ligands and methods i The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant inventive are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynecomastia, autoimmune disease, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prostate.
CN1869035A Lactone monomer compound and its application in preparing medicine for treating cancer A lactone monomer compound used for preparing the medicines to prevent and treat cancers, especially the liver cancer, is prepared from soursop seeds through drying, breaking, extracting in petroether, recovering petroether, laying aside to generate white deposit, filtering to obtain white deposit, chromatography by silicon gel column several times, and gradient eluting with petroether, petroether-ethyl acetate and ethyl acetate-methanol.
USRE38962 Diphenyl-triazole derivatives and their use as anti-gestative immuno-suppressant and anti-tumoral agents Compounds of formula (I), wherein X and Y are independently carbon or nitrogen but not both simultaneously carbon, R1 is a group (II) and R2 is a group (III), R5 being a carbonate, carbamate or phosphate residue, are useful as anti-gestative, immuno-suppressant and anti-tumor agents
CN101072780B Novel tetracyclic derivative containing heteroatoms useful as sex steroid hormone receptor modulators The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.
US20110104156 Methods and materials for treating autoimmune and/or complement mediated diseases and conditions Disclosed are methods for treating an autoimmune and/or complement mediated disease or condition in a subject. The methods include administering to the subject a compound which inhibits the subject's classical complement pathway. The methods include administering to the subject a compound which inhibits the subject's classical complement pathway. Compositions which include inhibitors of C1q, C1r, C1s, C2 or C4 and a pharmaceutically acceptable excipient are also described.
EP0869975B1 Assay for and uses of peptide hormone receptor ligands The invention features a method for determining whether a candidate compound is a non-peptide agonist of a peptide hormone receptor. In this method, a candidate compound is exposed to a form of the peptide hormone receptor which has an enhanced ability to amplify the intrinsic activity of a non-peptide agonist. The second messenger signaling activity of the enhanced receptor is measured in the presence of the candidate compound, and compared to the second messenger signaling activity of the enhanced receptor measured in the absence of the candidate compound. A change in second messenger signaling activity indicates that the candiate compound is an agonist. An increase in second messenger signaling activity indicates that the compound is either a full or partial agonist; a decrease in second messenger signaling activity indicates that the compound is an inverse agonist.
WO2013143299A1 Lactate-based fulvestrant or fulvestrant derivative oily preparation and preparation method thereof Fulvestrant or fulvestrant derivative oily preparation and preparation method thereof. The oily preparation comprises: fulvestrant or a fulvestrant derivative, the content being 10 mg/ml to 170 mg/ml; a lactate compound, the content being 5% to 80% of the total weight of the preparation; vegetable oil or artificially-synthetic oil (grease) ester; a pain-killer; and an optional antioxidant.
CN103191275A Pharmaceutical composition for treating serious thrush of equus animals The invention discloses a pharmaceutical composition for treating serious thrush of equus animals; the pharmaceutical composition comprises the components in parts by weight: 23-27 parts of salicylic acid powder, 4-6 parts of iodoform, 13-17 parts of alums, 23-27 parts of potassium permanganate powder, 8-12 parts of sulfanilamide powder and 18-22 parts of resina draconis powder; a using method of the pharmaceutical composition comprises the steps of: cleaning and soaking the hoof parts of the equus animals, and removing rotten cutin, surface excrescences and necrotic tissues; burning affected parts by hot vegetable oil; grinding the pharmaceutical composition into fine powder and then mixing the fine powder; dipping the medicine powder by a cotton ball and filling the medicine powder into the rotten parts, and covering sterilized gauze onto the rotten parts with the medicine powder; spreading pine tar outside the sterilized gauze, and padding gauze rolls; and binding bandage on the whole hoofs, and then spreading the pine tar. The pharmaceutical composition is organically combined, is dialectical in compatibility of medicines and enables the medicines to supplement with one another, and the effects of removing the rotten parts and regenerating new tissues as well as diminishing inflammation and stopping bleeding can be improved, so that the aim of curing the serious thrush can be achieved. The pharmaceutical composition is easy in material obtaining and convenient to prepare, reduces the drug residue and toxic and side effects, and is low in price and high in treatment effect.
CA2715036A1 Therapies for cancer using isotopically substituted lysine Methods of treatment and substances for treatment of cancer may use or cause the creation of isotopically modified lysine at levels that do not occur naturally.
CN101928270A Isobenzofuranone compound, preparation method thereof and use thereof The invention discloses a novel isobenzofuranone compound of a general chemical structural formula (I), a preparation method thereof and use thereof. In the formula, 1, 3, 4a, 4, 5, 6, 7, 7a, 8 and 9 represent C1, C3, C4a, C4, C5, C6, C7, C7a, C8 and C9 respectively; the isobenzofuranone compound is extracted from fungi of which the strain classification is cephalosporium AL031 and the strain collection number is CCTCC No.M2010140. The compound is subjected to antioxidant activity and antitumor activity screening. Experiment results show that the compound has high antioxidant activity and antitumor activity and a promising medicinal application prospect.
US20120238549 Nuclear Hormone Receptor Modulators The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
CN103664986A Antineoplastic compound extracted from gamboges, preparation method and application of antineoplastic compound The invention relates to an antineoplastic compound extracted from gamboges, a preparation method and application of the antineoplastic compound. The antineoplastic compound is prepared through the following steps: (1) using ethyl acetate to perform extraction on gamboges, performing silica gel column chromatography separation and petroleum ether-ethyl acetate gradient elution on the extractive to obtain components A to K; (2) eliminating grease component and gambogic acid component, and performing repeated analysis via HPLC-PDA-MS to obtain component I; (3) performing silica gel column chromatography separation and chloroform-methyl alcohol gradient elution on the component I to obtain fraction I-3; (4) performing RP-18 chromatograph separation and acetonitrile-water gradient elution on the fraction I-3 to obtain sub-fraction I-3C; (5) performing purification and acetonitrile elution on the sub-fraction I-3C to obtain the antineoplastic compound. The antineoplastic compound can be used for treating tumours.
CN102382054A Parazole and isoxazole derivative, preparation method for same and application thereof The invention discloses a parazole and isoxazole derivative, a preparation method for same and application thereof. The parazole and isoxazole derivative prepared by the method is higher in survivability and specificity and is a novel candidate drug for male contraception in clinic, thereby having higher application value. The parazole and isoxazole derivative is a compound with the general constitutional formula I.
WO2009151329A1 Nutrition for prevention of infections A nutritional composition comprising a combination of non-digestible oligosaccharides and a product obtained by incubating an aqueous substrateby bifidobacteria and optionally a product obtained by incubating an aqueous substrate by S. thermophilus. Said combination reduces bacterial translocation and improves the intestinal barrier function.
WO2014143201A1 Method for noribogaine treatment of addiction in patients on methadone A short treatment with noribogaine shows promise for treating drug dependency. Many opioid addicts are treated with methadone. We have found that giving noribogaine to mammal concurrently being administered methadone surprisingly exacerbates methadone's negative side-effects, and increases the risk of death. Therefore, prior to noribogaine treatment, a patient on methadone therapy undergoes a period of methadone abstinence to wash out the methadone. Surprisingly, noribogaine does not react negatively to morphine. Therefore, the methadone regimen is replaced with morphine prior to noribogaine treatment.
EP1793819A2 Carbazole and cyclopentaindole derivatives to treat infection with hepatitis c virus The invention is directed to a method of treating, preventing, or inhibiting a Hepatitis C viral infection in a mammal comprising contacting the mammal with an effective amount of a compound of the formula (I) wherein substitutions at R1 - R13, m and Y are set forth in the specification
CN101367853A 13-membered azalides and their use as antibiotic agents The invention relates to a method of preparing compounds of formula (1) and pharmaceutically acceptable salts thereof. The compounds of formula (1) are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula (1) and methods of treating bacterial protozoa infections by administering the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1) and intermediates useful in such preparation.
CN102697726A Liposome combined medicament of alprostadil and like and large-scale industrial production technology and application thereof The invention relates to a liposome combined medicament of alprostadil and the like, large-scale industrial production technology and applications thereof, and is characterized in that a raw material molar ratio of components of the liposome combined medicament of alprostadil and the like of the invention is disclosed; the invention also provides a large-scale industrial preparation method of the liposome combined medicament, which is characterized in that according to pharmaceutically-allowable dosages, freeze-dried injection, or oral preparations, or sprays, or suppositories of the liposome combined medicament of alprostadil and the like are prepared; the liposome combined medicament of alprostadil and the like is characterized in that the applications comprise virus resistance, tumor resistance, angina resistance, and blood pressure reduction.
CN102091026A Externally applied antithyroid gel and preparation method thereof The invention provides an externally applied antithyroid gel. The externally applied antithyroid gel comprises a medicament, a macromolecular substrate material, a solvent, a cosolvent, a humectant and a preservative, and selectively contains any of an antioxidant, a neutralizer and a penetration enhancer. Defects of the traditional curative medicament are overcome by the externally applied antithyroid gel. When smeared on a neck lesion site, the antithyroid gel has high absorption effect, obvious treatment effect and no obvious side effect for the whole body, and is suitable for mass production. Particularly, no trace or residue is left on the smeared part after the antithyroid gel is smeared or absorbed. When the antithyroid gel is used for treating hyperthyroidism, the repeated incidence and the relapse rate are low, the treatment effect on hyperthyroidism is improved, and pains of patients are alleviated.
CN101429198A Banisterine derivant and uses thereof The invention relates to a yageine derivative and salts of compounds. The invention synthesizes the novel yageine derivative compounds which can strengthen the antineoplastic activity and reduce the toxicity of a nervous system through the structural modification to locus 1, 2, 3, 7 and 9 of beta-carboline parent nuclei of yageine. The compounds can be used for preparing drugs used to treat various tumor diseases through the screening study of in vivo and in vitro anti-tumor experimental models.
WO2014079154A1 Benzo five-membered nitrogen heterocyclic piperidine or piperazine derivatives and preparation methods and pharmaceutical compositions thereof The present invention relates to the compounds of formula (I) or pharmaceutically acceptable salts thereof: wherein R1, R2, X, Υ, Α and Β are defined in the description. Also disclosed in the present invention are the methods for preparing the compounds of formula (I) or pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the compounds of formula (I) or pharmaceutically acceptable salts thereof.
US20080221071 Comprises lumisterol and tachysterol, for topical administration Methods for enhancing the ability of an individual, exposed to sunlight, to produce vitamin D via the skin. Pharmaceutical compositions comprising provitamin D and at least one of lumisterol and tachysterol and analogs and derivatives thereof are also disclosed.
CN102000086A Application of asiatic acid in preparing medicament for treating or preventing pancreatic fibrosis The invention discloses application of asiatic acid in preparing a medicament for treating or preventing pancreatic fibrosis. By Influence of the asiatic acid to rat pancreatic fibrosis, the invention proves that the asiatic acid has the function of resisting the pancreatic fibrosis. Therefore, the asiatic acid can be used as an active component to prepare the medicament for resisting the pancreatic fibrosis.
US20120121700 Pharmaceutical formulations comprising valganciclovir Pharmaceutical formulations prepared by granulating valganciclovir or a salt thereof, using a nonaqueous solvent or hydro-alcohol.
CN101209251A Elastic nano vesicle preparations containing paclitaxel or docetaxel and preparation thereof The invention pertains to the technical field of medicine, which more particularly relates to an elastic nano-vesicle preparation used for transitting the active ingredient paclitaxel (taxol) or docetaxel to penetrate the natural permeability barriers or pores (such as, skin, mucosa, tissues and organs, etc.) and a preparation method thereof. The preparation at least contains the following components with the weight percentages: 3 to 15 percent of phospholipid, 0.3 to 5 percent of sodium cholate or sodium deoxycholate, 0.01 to 5 percent of paclitaxel or docetaxel, 5 to 30 percent of alcohol and the rest of water or phosphate buffer solution. The formed elastic nano-vesicle has lipid double molecular layers, and the diameter of the typical elastic nano-vesicle is less than 200nm. The preparation is used for the treatment of malignant tumors, and the invention can be taken by injection, spray or transdermal drug delivery.
WO2011126409A1 Telomerase inhibitors and a method for the preparation thereof The invention relates to the fields of organic and medicinal chemistry, and molecular biology, and concerns a method for the preparation of a new class of telomerase-inhibiting compounds, which can be utilized for studying telomerases and catalytic sub-units of telomerases, and reverse transcriptases, and for studying and treating neoplastic and viral diseases. Telomerase-inhibiting coordination compounds of derivatives of imidazol-4-one are characterized by general formula (1).
EP1767215A1 Isoflavones against radiation-induced mortality The present invention provides compositions and methods for the prophylactic and therapeutic treatment of animals, including humans from radiation injury. In particular, the present invention provides methods and compositions comprising the isoflavone genistein (4', 5, 7-trihydroxyflavone) or phytoestrogenic isoflavonoids.
US20100075923 Method of enhancing tgf-beta signalling The present invention is directed to a method of enhancing TGF-β signaling in a subject comprising administering to said subject a clathrin-dependent endocytosis inhibitor in an amount sufficient to enhance TGF-β signaling. In another aspect, the invention is directed to a method of treating a condition associated with decreased TGF-β signaling in a patient in need thereof comprising administering to said patient a clathrin-dependent endocytosis inhibitor in a therapeutically effective amount.
WO2014079150A1 Compounds and their methods of use Provided are compounds of formula (I), which can inhibit glutaminase. Pharmaceutical compositions comprising these compounds and uses as glutaminase inhibitors for treating cancers thereof are also provided.
US20100144700 Heterocyclic-carbonyl-diazabicycloalkanes as modulators of the neuronal nicotinic acetylcholine alpha 4 beta 2, subtype receptor for the treatment of cns related disorders A compound of Formula 1: A-C(O)-Cy, wherein A is a diazabicyclic core, containing 7, 8, or 9 ring atoms, and selected from the following: 2,6-diazabicyclo[3.2.0]heptane; 3,6-diazabicyclo[3.ZO]heptane; 2,7-diazabicyclo[4.2.0]octane; 3,7-diazabicyclo[4.2.0]octane; 3,8-diazabicyclo[4.2.0]octane; 2,7-diazabicyclo[3.3.0]octane; 2,7-diazbicyclo[4.3.0]nonane; 2,8-diazbicyclo[4.3.0]nonane; 3,7-diazabicyclo[4.3.0]nonane; 3,8-diazabicyclo[4.3.0]nonane; 3,9-diazabicyclo[4.3.0]nonane; 2,6-diazabicyclo[3.2.1]octane; 3,6-diazabicyclo[3.2.1]octane; wherein the diazabicycle is attached as a radical to the depicted carbonyl via either one of the two ring nitrogen atoms, such that the carbonyl forms an amide bond with the ring nitrogen; Cy is a heteroaryl group; The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α402 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds are believed to: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects, namely side effects such as significant Increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle.
CN103476412A Aclidinium for use in improving the quality of sleep in respiratory patients The present invention provides aclidinium or any of its steroisomers or mixture of stereoisomers, or a pharmaceutically acceptable salt or solvate thereof, for improving the quality of sleep in respiratory patients.
CN1587265A 10-alkoxy camptothecine derivative and its preparing method and use The present invention discloses 10-alkoxy camptothecinie derivatives and its preparation process and application in treating tumor. The compounds have extraneous antitumor activity in different degree to P388 human leukemia cell, A649 human lung cancer cell, PC-3 human prostate cancer cell, HO-8910 human oophoroma cell, and K562 and HL60 human leukemia cell. The experiment of inoculating naked mouse with transplanted PC-3 human prostate cancer cell and inoculating mouse with S180 malignant solid tumor shows that partial compounds possess powerful tumor inhibiting activity.
US20110217249 Compositions and Methods for the Treatment of Skin Diseases and Disorders Using Antimicrobial Peptide Sequestering Compounds The present invention provides compositions containing one or more antimicrobial peptide sequestering compounds and methods for topical application of such compositions to the skin to treat skin diseases and disorders such as rosacea in humans.
CN103446040A Docetaxel-coated polymeric micelle and preparation method thereof The invention belongs to the technical field of biological medicines, and relates to a docetaxel-coated polymeric micelle and a preparation method thereof. The preparation method is characterized in that a thin-film dispersion method is used for preparing a docetaxel Pluronic F127/P105 mixed micelle, Pluronic is used as a carrier, and docetaxel is coated in a hydrophobic inner core PPO (poly-p-phenylene oxide) of Pluronic. The mixed micelle prepared by the method can be used for effectively improving the solubility of the docetaxel; the PEO (polyoxyethylene) long chain of F127 can play a role in long circulation and is prevented from being phagocytized by a reticulo-endothelial system, thus the half-life period of the mixed micelle in blood is prolonged; the P105 in the mixed micelle can be used for inhibiting the excretion of P-gp to the maximum degree and can efficiently reverse the multidrug resistance of tumors so as to improve the treatment effect on the tumors. The mixed micelle prepared by the method does not contain Tween-80 or alcohol. Compared with commercially available docetaxel injection, the mixed micelle can be used for obviously improving the toxic and side effects of the medicines and the safety of clinical application.
CN1965813A Compound soft capsule of propolis Disclosed is a composite bee glue soft capsule which comprises (by weight percent) bee glue liquid 28-36%, fish oil 58.8-66.8%, bee wax 2-3%, shortening 2-3%, vitamin E 0.1-0.3%. The soft capsule has the functions of lowering blood fat and improving human body immunity.
US6977270 Tocotrienolquinone cyclization product with an anti-hypercholesterol effect A description is given of the use of at least one compound of the formula I where R1, R2, R3 and R4 independently of one another are H or C1-C6-alkyl; and the use of a compound of the formula I for medical use.
CN1796402A Technique for preparing general alkaloid of Hubei fritillary bulb This invention publishes a preparation technique for alkaloids in Hubei bulbus fritillariae, which includes medicinal materials preprocessing, ethanol refluxing, condensation, purification, impurity removal, on-column purification and vacuum desiccation. In ethanol refluxing, a water-containing ethanol solution with proper concentration is adopted, while in on-column purification, macroporous adsorption resin purification technology is employed. This technique is free from organic solvents such as chloroform and ethyl acetate during fritillaria alkaloid extraction, and therefore, the product quality is promoted while the production period is reduced, which is suitable for industrial production.
CN102924421A Preparation method and application of compound having tyrosinase inhibitory activity The invention provides a preparation method of a compound having tyrosinase inhibitory activity. The compound comprises six polyphenols extracted from mulberry leaves and having the tyrosinase inhibitory activity. Medicinal materials are subjected to heating and extraction through an ethanol water solution, concentration, silicagel column separation, elution and concentration and drying through an elution solution and then are subjected to continuous separation through preparative liquid chromatography, and a solution is collected, concentrated and dried to obtain a sample and then is subjected to structural identification. The invention further provides a method for separating the polyphenols from the mulberry leaves. The six polyphenols have strong tyrosinase inhibitory activity and can effectively prevent and treat human body chromatosis diseases and melanoma caused by abnormal melanin synthesis and other diseases needing to inhibit the tyrosinase inhibitory activity, and the preparation method can be used for preparing pharmaceuticals for treating the diseases.
WO2013165592A1 Treatment of latent hiv infection Methods for treating HIV positive patients, and purging and eradicating latent HIV virus from a patient's system, are disclosed. The bulk of viral load is eradicated using conventional antiretroviral (ARV) therapy. Compounds that encourage viral production in the latent cells are then administered, preferably without activating those cells, while maintaining the ARV therapy. The administration of compounds that encourage viral production in latent cells is cycled, and after around 7-10 cycles, the methods can virtually eliminate latent HIV in the patient. Ideally, the ARV regimen includes at least one integrase inhibitor, at least one entry inhibitor, such as a CCR5 antagonist, and at least one, and preferably two, reverse transcriptase inhibitors. The compounds that encourage viral production in latent cells ideally include a combination of prostratin or a prostratin analog and an HDAC inhibitor, such as butyrate, valproate, or SAHA.
US20070280930 Cd44-Targeting for Reducing/Preventing Ischemia-Reperfusion-Injury The present invention relates to CD44 binding molecules, preferably anti-CD44 antibodies, and their use in methods for the prevention or reduction of ischemia-reperfusion injury in e.g. solid organ transplantation or in patients in shock. The invention further relates to methods wherein levels of soluble CD44 are determined in e.g. serum or urine as a prognostic factor for the risk of organ rejection.
WO2010065329A2 Nanoparticles for cancer treatment Methods and composition for improving therapeutic potential of isothiocyanate. For example, in certain aspects methods for preparing a composition containing an isothiocyanate nanoparticle formulation and uses thereof are described. Furthermore, the invention provides such a composition.
US20080113899 Iron Supplement and Utilization of the Same The present inventors have found that a siderophore-iron (III) ion chelate complex is highly absorbed in the body; significantly increases the blood hemoglobin concentration, the serum iron concentration and the concentration of iron stored in the liver; and causes no adverse effects on the body. On the basis of these findings, the present inventors provide iron supplementing agents, agents for the prevention or treatment of iron defeciency anemia, food additives and food compositions, each of which contains a siderophore and iron (III) ions, preferably in the form of a chelate complex.
WO2007017244A3 A PROCESS FOR THE PURIFICATION OF SUBSTITUTED 2-(2-PYRIDYLMETHYL)SULFINYL-lH-BENZIMIDAZOLE COMPOUNDS BY PRECIPITATION IN THE PRESENCE OF A QUATERNARY AMMONIUM SALT A process for the preparation of substituted 2-(2-pyridylmethyl) sulfinyl-1H- benzimidazoles compounds from a suitable solvent or a mixture of solvents in the presence of a quaternary ammonium compound.
US20050032900 For topical administration, without the presence of conventional oil in water (O/W) emulsifying agent; percutaneous delivery of ibuprofen is improved by using a skin penetration enhancer, such as 2-n-nonyl-1,3-dioxolane or decanal, dimethyl acetal, as the oily phase of the emulsion Emulsions and creams containing ibuprofen effective for topical administration of the ibuprofen are provided without the presence of conventional O/W emulsifying agent. The emulsions and creams are formed by using the ibuprofen, in the form of its salt, as the O/W emulsifying agent. A minor amount of a W/O emulsifying agent may be included in the composition. Percutaneous delivery of ibuprofen is improved by using a skin penetration enhancing compound, such as 2-n-nonyl-1,3-dioxolane or decanaldimethyl acetal, as the oily phase of the emulsion.
US20090257983 Medical treatment device for treating aids by utilizing modified human immunodeficiency virus virions to insert anti-viral medications into t-helper cells The medical device by which a modified Human Immunodeficiency Virus or virus-like structure is used as a transport medium to carry a payload of a quantity of anti-viral drug molecules to T-Helper cells in the body. The modified Human Immunodeficiency Virus or virus-like structure makes contact with a T-Helper cell by means of the modified virus's exterior probes or virus-like structure's exterior probes. Once the exterior probes engage the T-Helper cell's receptors, the modified virus or virus-like structure inserts into the T-Helper cell the quantity of medically therapeutic anti-viral drug molecules it is carrying. The anti-viral drug molecules exhibit an anti-viral effect when present inside the T-Helper cells thus assisting in repelling an infection by the Human Immunodeficiency Virus and the use of such a device significantly lowers the occurrence of unwanted deleterious side effects.
US20080242658 Inhibitors of Iap Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I
US7384925 2' Hydroxy-3'-bromo-3,4,4',5-tetramethoxy-(Z)-stilbene; antimitotic agent; inhibits the assembly of tubulin into microtubules; anticarcinogenic: solid tumor cancers, neovascularization; tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and A-4 (extract from willow tree) Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.
US8247400 Cephem compounds useful for the treatment of bacterial infections The present invention relates to new cephem compounds useful for the treatment of bacterial infections of formula I: The invention also relates to methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and to methods of treatment using the compounds. The new cephem compounds are stable, exhibit good solubility, and are particularly well suited for, e.g., parenteral administration for the treatment of bacterial infections.
CN102784381A Clinical scientific prescription for treating cataract The invention provides a clinical scientific prescription for treating cataract, belonging to the medical field. The clinical scientific prescription is characterized by being prepared by six ingredients which are respectively calcium, ferrum, selenium, protein, fetal bovine bone marrow and spirulina, and is characterized by the following formula: 7.8% of calcium, 8.51% of ferrum, 0.00124% of selenium, 46.8% of protein, 8.51% of fetal bovine bone marrow and 28.36% of spirulina; and the sum of the six ingredients is 7052.09mg.
WO2011120153A1 Compounds and method for treatment of hiv The invention relates to a compound of Formulae I and/or II: Formula I Formula II and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof; X is selected from Se, N-OH, NH, NO2, CN, N-CN, N=O, O or S, and the remaining substituents are described herein; and a composition thereof. The invention also relates to a method of administration thereof; and use thereof to treat HIV.
EP1511723A1 Sulfone liver x-receptor modulators The present invention is directed to slective LXR modulators, small molecule compounds corresponding to Formula (I) wherein: R1 and R2 are independently hydrogen or optionally substituted alkyl, alkenyl, aryl, acyi, or alkaryl; R3 is optionally substituted alkyl or aryl; each R4 is independently hydrogen, alkyl, aryl,.heteroaryl, hydroxy, alkoxy, cyano, nitro, amino, alkenyl, alkynyl, amido, alkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, haloalkylcarbonyl, alkylthiocarbonyl, arylthlocarbonyl, alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxyl, haloalkyl, cyano, nitro, carboxyl, amino, alkoxy and aryl, or aryl optionally substituted with one or more substituent selected from hydrogen, halogen, haloalkyl, hydroxy, lower alkyl, alkoxy, methylene dioxy, ethylenedioxy, cyano, nitro, atkylthio, alkylsulfonyl, sulfonic acid, sulfonamide, carboxyl derivatives, amino, aryl and heteroaryl; and a is 0-4, and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.
US20050214761 For introducing DNA into organisms which produce large amounts of oils and, in particular, oils with a high content of unsaturated fatty acids The invention relates to a novel elongase gene with the sequence SEQ ID NO:1 or its homologs, derivatives or analogs, to a gene construct comprising this gene or its homologs, derivatives and analogs, and to its use. The invention also relates to vectors or organisms comprising an elongase gene with the sequence SEQ ID NO:1 or its homologs, derivatives or analogs. Furthermore, the invention relates to a process for the preparation of polyunsaturated fatty acids and to a process for introducing DNA into organisms which produce large amounts of oils and, in particular, oils with a high content of unsaturated fatty acids. Moreover, the invention relates to an oil and/or a fatty acid preparation with a higher content of polyunsaturated fatty acids with at least two double bonds and/or a triacylglycerol preparation with a higher content of polyunsaturated fatty acids with at least two double bonds.
US20080286280 Stable Lyophilized Pharmaceutical Preparations of Monoclonal or polyclonal antibodies The invention concerns lyophilized pharmaceutical preparations of monoclonal or polyclonal antibodies which contain a sugar or an amino sugar, an amino acid and a surfactant as stabilizers. In addition the invention concerns a process for the production of this stable lyophilisate as well as the use of a sugar or amino sugar, an amino acid and a surfactant as stabilizers for therapeutic or diagnostic agents containing antibodies.
WO2014108899A1 Fluorinated cbd compounds, compositions and uses thereof The present invention relates to fluorine substituted CBD compounds, compositions thereof and uses thereof for the preparation of medicaments.
CN101518538A Application of tanshinone compound used as specific inhibitor for CYP1 family The invention relates to the field of natural medicaments, in particular to a diterpenes compound in a radix salviae miltiorrhizae extract, mainly relates to the expression of a tanshinone compound in a reversal benzoapyrene-induced CYP1 enzyme, as well as application in the direct inhibition of the CYP1 enzyme activity. The invention discloses new pharmacological application of four types of tanshinones including tanshinone I, tanshinone II A, cryptotanshinone and dihydrotanshinone I, namely the four tanshinones not only can directly inhibit the activities of various subtype enzymes in the CYP1 family but also can reverse the up-regulation of a benzoapyrene-induced CYP1 function in Hep-G2 cells. The tanshinone compound has the development application prospect that the tanshinone compound can be developed into a supplementary drug for the treatment of cancer as a multi-drug resistant reversal agent and an anti-cancer health care product.
EP1085900B1 Use of erythropoietin for the treatment of primary haemochromatoses The invention relates to the use of Epo for the production of pharmaceutical preparations for the treatment of haemochromatoses and pharmaceutical combination preparations containing erythropoietin (Epo) and calcium and/or phosphate compounds. These combination preparations are used particularly for the treatment of primary haemochromatoses.
US7897595 Pyridoazepine derivatives The present invention relates to pyridoazepine derivatives that act as 5-HT ligands, e.g., 5-HT2 C. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
WO2004089943A8 Antimicrobial [3.1.0] bicyclohexylphenyl-oxazolidinone derivatives and analogues The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formula (I) or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
US20070275984 Novel Thieno-Pyridine and Thieno-Pyrimidine Derivatives and Their Use as Positive Allosteric Modulators of Mglur2-Receptors The present invention relates to novel compounds, in particular novel thieno-pyridine and thieno-pyrimidine derivatives according to Formula (I), wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
WO2005085443A3 Rnai-based therapeutics for allergic rhinitis and asthma The present invention provides compositions comprising one or more RNAi agents (e.g., siRNAs, shRNAs, or RNAi vectors) for the treatment of conditions and diseases mediated by (e.g., featuring IgE-mediated hypersensitivity), as well as systems for identifying RNAi agents effective for this purpose. The compositions are suitable for the treatment of allergic rhinitis and/or asthma. In certain embodiments of the invention the RNAi agent is targeted to a transcript that encodes a protein selected from the group consisisting of the FCϵRIα chain, the FCϵRIβ chain, c-Kit, Lyn, Syk, ICOS, OX40L, CD40, CD80, CD86, RelA, RelB, 4-1BB ligand, TLR1, TLR2, TLR3,TLR4, TLR5, TLR6, TLR7, TLR8, TLR9, CD83, SLAM, common Ϝ chain, and COX-2. In addition, the invention provides RNAi agent/delivery agent compositions and methods of use. In certain embodiments of the invention compositions comprising an RNAi agent are delivered by the respiratory route.
CN101164556A Musk ointment for treating osteopathy The present invention relates to a musk ointment for curing osteopathy. Said musk ointment can be effectively used for curing the diseases of osteomyelitis, osteonecrosis, bone tuberculosis, lymphoid tuberculosis, hyperplasia of cervical vertebrae, prolapse of lumbar intervertebral disk and traumatic injury, etc. said musk ointment is made up by using musk, borneol, minium, dahurian angelica root, myrrh, charred hair, used old lime, yellow wax and pure sesame oil through a certain preparation process. Said invention also provides the concrete steps of its preparation process.
WO2010123156A1 Angiogenesis inhibitor Disclosed is a novel composition which has an effect of inhibiting or preventing angiogenesis, is applicable to the treatment, prevention or recurrence prevention of diseases associated with an angiogenic mechanism such as diabetic retinopathy and age-related macular degeneration, and is an alternative for physical therapies. Specifically disclosed are: an angiogenesis inhibitor comprising an inhibitor of CD9 that belongs to a four transmembrane protein family; and an anti-angiogenic composition comprising the angiogenesis inhibitor.
WO2008081096A3 Quinolinyl derivatives, method for preparing same, pharmaceutic compositions containing same, and use thereof as hypoglycemiant and hypolipemiant agents The invention relates to compounds of the formula (I) in which : R1 is an alkyl group substituted or unsubstituted with one or more COOR3 or NR4R5 groups; R2 is a substituted or unsubstituted phenyl group; and n is 0, 1, 2, 3, 4, 5, 6, 7 or 8. Use in drugs.
CN102846642A Veterinary drug for treating gram-positive bacteria of fowl, and its preparation method The invention discloses a veterinary drug for treating gram-positive bacteria of a fowl, and is characterized in that the veterinary drug comprises aureomycin, procaine penicillin, sulfamethazine and starch. The inventive veterinary drug can effectively treat symptoms of fowl caused by gram-positive bacteria, has evident curative effect, is convenient to use and can be widely popularized.
US20090215800 Enzyme and Receptor Modulation Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.
US20100249200 Novel Compounds 569 The present invention provides compounds of formula (I) wherein Ra, Rb, R1, R2, R3, R4, R5, R6 and R29 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
CN103169711A Solid dosage forms of valsartan, amlodipine and hydrochlorothiazide and method of making same The invention relates to solid dosage forms of valsartan, amlodipine and hydrochlorothiazide and a method of making the same, and also relates to monolayer, bilayer and trilayer solid dosage forms of a combination of valsartan, amlodipine and hydrochlorothiazide.
US20110224224 Method of Optimizing the Treatment of Philadelphia-Positive Leukemia with Imatinib Mesylate The present invention relates to a method of treating Philadelphia-positive leukemia (Ph+ leukemia), in a particular chronic myeloid leukemia (CML), in a human patient population. More specifically, the present invention pertains to a method of treating Ph+ leukemia, such as CML or Ph+ ALL, in a human patient suffering from Ph+ leukemia comprising the steps of (a) administering a predetermined fixed amount of Imatinib as a free base or in the form of a pharmaceutically acceptable salt thereof to the human patient, (b) collecting at least one blood sample from the patient, e.g. within the first 12 months of treatment, (c) determining the plasma trough level (Cmin) of Imatinib, (d) determining the OCT-1 Activity in the blood sample, and (e) adjusting the dose of Imatinib applied to the individual patient in a manner that an Imatinib Cmin value is achieved in the patient of at least 800 ng/mL, if in step (c) an Imatinib Cmin value of less than 800 ng/mL is found and in step (d) an OCT-1 Activity is found below 6.0 to 10.0 ng/200,000 cells.
US20080188510 Novel methods using zonisamide The present invention relates to usefulness of zonisamide as a pharmaceutical composition for treating dementia or cognitive impairment.
EP1890700A2 Methods and compositions for managing psychotic disorders Compositions for treating psychotic disorders comprise a first ingredient and a second ingredient, wherein the first ingredient comprises at least one antipsychotic agent selected from the group consisting of ziprasidone, olanzapine and risperidone and the second ingredient comprises at least one anticonvulsant selected from the group consisting of zonisamide and topiramate. Methods of treating psychotic disorders, symptoms associated with psychotic disorders, and side effects associated with antipsychotic agents, comprise administering a first ingredient and a second ingredient, wherein the first ingredient comprises at least one antipsychotic agent selected from the group consisting of ziprasidone, olanzapine and risperidone and the second ingredient comprises at least one anticonvulsant selected from the group consisting of zonisamide and topiramate. The second ingredient of the compositions and methods may further comprise an antidepressant. In various embodiments, the antipsychotic agent and the anticonvulsant act synergistically to alleviate symptoms and/or side effects associated with psychotic disorders and their treatment.
WO2014100765A1 Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.
EP2176208A1 Prodrugs of cannabidiol, compositions comprising prodrugs of cannabidiol and methods of using the same Described herein are cannabidiol prodrugs, methods of making cannabidiol prodrugs, formulations comprising cannabidiol prodrugs and methods of using cannabidiols. One embodiment described herein relates to the transdermal or topical administration of a cannabidiol prodrug for treating and preventing diseases and/or disorders.
CN101015638A Bone recovering plaster The invention discloses a plaster for treating bone diseases, wherein the raw materials include mulberry branch and root, willow branch, pagoda tree peel, grape root, bark of peony root, jasmine root, elm bark, pine bark, scrophularia root, pubescent angelica root, dahurian angelica root, Chinese angelica root, frankincense, myrrh, arisaema tuber, stinkweed, sesame oil, yellow lead and far infrared powders. The plaster is prepared through steps of squeezing, extracting, immersing and heating.
EP1984362B1 Process for preparing intermediates to 5-ht4 receptor agonist compounds The invention provides 8-azabicyclo[3.2.1]octyl intermediates of formula (I): useful for the preparation of 5-HT4 receptor agonist compounds. The invention also provides processes for the preparation of such useful intermediates.
WO2009152210A3 Coumarin compounds and their use for treating cancer Coumarin compounds are disclosed herein. Also disclosed is a method for treating cancer with coumarin compounds.
US20100292338 Silk medical device with antimicrobial properties and a method of manufacture thereof A silk medical device is described, which is useful for the treatment of wounds to prevent infection. The silk medical device is manufactured from a silk protein material that is loaded with a polymeric cationic antimicrobial, such as polyhexamethylene biguanide (PHMB).
US20060233738 Composition for promoting production of type 1 collagen and/or elastin This invention aims to provide a composition that promotes the production of type I collagen and/or elastin in the human skin fibroblast cells, wherein the composition improves the suppleness and elasticity of the skin, is amply effective in preventing and improving wrinkles and sagging, and is also very safe to the skin. The present invention relates to a composition that contains silymarin, which is a general term for flavonolignans such as silybin, silydianin, silychristin and isosilybin, wherein the aforementioned composition has a property to promote the production of type I collagen and/or property to promote the production of elastin. It also relates to a composition containing silymarin derived from a silymarin-containing plant and/or extract of such plant, wherein the aforementioned composition also has a property to promote the production of type I collagen and/or property to promote the production of elastin.
CN101402619A Novel 2-deoxidizedfructofuranose derivative, preparation method and medical uses thereof The invention discloses a novel micromolecule capable of inhibiting and killing tumor cells, a method for preparing a medical preparation of the micromolecule, and application thereof. The structure is shown in general formula (I), wherein R1, R2, R3, R4 and R5 are defined as in the instruction. The compound is used for treating cancers.
US20110183980 O-benzyl nicotinamide analogs as mglur5 positive allosteric modulators In one aspect, the invention relates to O-benzyl nicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
US20080287459 Pharmaceutical Composition for Treating Hair Loss and Benign Prostatic Hyperplasia The present invention is related to an orally administered pharmaceutical composition for the prevention of hair loss; having the effects of epilation, hair toning, and hair growth; and for the treatment of female hirsutism and benign prostatic hyperplasia. The composition of the present invention is non-steroidal and is advantageous in that it has no side effects such as lowering of sexual function, etc. shown in the conventional oral treatment agents of related diseases.
CN101444495B Vitamin E microcapsule preparation method A vitamin E microcapsule preparation method belongs to the technical field of preparation of controlled-release microcapsule for food additives and bioactive substances. The vitamin E microcapsule preparation method can improve the stability of vitamin E and amplify the application range. The method comprises the following steps: selecting chitosan and maltodextrin as wall material, selecting soybean lecithin (P powder) and Tween-80 as the composite emulsifying agent; and synthesizing vitamin E microcapsule by spray drying. The vitamin E microcapsule has embedding rate up to 92.45%, retentionrate up to 91.73%, and water content lower than 3%, and has wide application prospect in the fields of bread or snack products, beverages, biscuits, health products and nutrient fortified food, etc. The method has the advantage of low cost and simple process, can meet the environmental protection and practical requirement.
CN102764396A Black plaster The invention discloses a black plaster which is prepared of, by weight, 8000 grams to 9000 grams of balm, 5600 grams to 6000 grams of minium, 80 grams to 100 grams of pseudo-ginseng, 150 grams to 160 grams of alums, 150 grams to 160 grams of ligusticum chuanxiong hort, 230 grams to 150 grams of motherwort herb, 100 grams to 120 grams of giant knotweed rhizome, 130 grams to 150 grams of myrrh, 50 grams to 7o grams of rhizoma sparganii, 100 grams to 200 grams of leech, 150 grams to 200 grams of gastrodia elata, 180 grams to 200 grams of white silkworm, 150 grams to 170 grams of Japanese thistle herb, 50 grams to 70 grams of cinnamon and 230 grams to 250 grams of bletilla. The black plaster has high adhesive strength and can be recycled, the efficacy can last for 40 days, and the black plaster can cure diseases of slipped discs, various waist and leg pains, cervical spondylosis, rachitis, osteoproliferation, scapulohumeral periarthritis, ulcerative carbuncle, mumps,trauma infections, broken bone setting, chronic pains, festering and the like.
EP1641444A1 Treatment of muscle fatigue The present invention involves the use of a compound that reduces the level of free fatty acids circulating in the plasma of a subject in the manufacture of a medicament for the treatment of prevention of muscle (particularly cardiac or skeletal muscle) impairment or fatigue.
WO2006100026A8 2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl-piperidines used as cgrp antagonists The invention relates to novel CGRP antagonists of general formula (I), in which B, R1 and R2 are defined as cited in claim 1, to their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts, in addition to the hydrates of their salts, in particular their physiologically compatible salts, with inorganic or organic acids or bases. The invention also relates to medicaments containing said compounds, to their use and to a method for their production.
US20070054886 Ras antagonists for treating neurodegenerative disorders Disclosed are methods of neuroprotection or treatment of neurodegenerative disorders with Ras antagonists.
CN103272039A Nano-silver gynecological effervescent tablet The invention discloses a nano-silver gynecological effervescent tablet, which comprises menthol radix sophorae flavescentis, acetic chlorhexidine, sodium bicarbonate, lithospermum, golden cypress and spina gleditsiae. The nano-silver gynecological effervescent tablet disclosed by the invention has the main functions of clearing away heat, drying dampness, promoting blood circulation to restore menstrual flow, clearing toxic materials and relieving itching, has high disintegration speed, plays effects quickly and is uniformly distributed in cervix uteri and vagina, can go deep into mucosa wrinkles, and has the advantages of being absorbed completely, causing no damage to mucosa, and being clean, sanitary and easy to store, etc.
US20120213769 Methods of diagnosing amyotrophic lateral sclerosis (als) A method of diagnosing amyotrophic lateral sclerosis (ALS) in a subject in need thereof is provided. The method comprising determining in cells of the subject at least one alteration in a sequence or expression level of Cytoplasmic FMR Interacting Protein (CyFIP2; Accession AF160973) and/or Retinoblastoma Binding Protein 9 (RbBP9; Accession AF039564), wherein an altered sequence or expression of the sequence or expression level of the CyFIP2; Accession AF160973) or Retinoblastoma Binding Protein 9 (RbBP9; Accession AF039564) as compared to a control reference sample from a non-ALS subject, is indicative of ALS. The present teachings may be implemented in screening for novel anti-ALS medicaments and for treating ALS.
EP1228087B1 Antibody catalysis of enantio- and diastereo-selective aldol reactions Nine efficient aldolase antibodies were generated using hapten 2. This hapten combines, in a single molecule, structural components employed for reactive immunization with structural components employed for forming a transition state analog of the aldol reaction. Characterization of two of these antibodies reveals that they are highly proficient (up to 1000-fold better than any other antibody catalyst) and enantioselective catalysts for aldol and retro-aldol reactions and exhibit enantio- and diastereo- selectivities opposite that of antibody 38C2.
US20050020630 Antiinflammatory agents; cardiovascular disorders; anticancer agents; antiarthritic agents; skin disorders; autoimmune disease; cardiovascular disorders The present invention provides benzo[b]thiophenes of Formula I: wherein R1, R2, R3, and L have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
CN1594316A Substituted pyrazolone derivatives and their preparing process and pharmaceutical conpositions Disclosed is a pyrazolone derivative having blood sugar lowering action represented by formula (I), wherein R1 is hydrogen or low level alkyl or low level alkoxy, R2, R3, R4, R5 are separate hydrogen atom, halogen, low level alkyl, low level alkoxy, hydroxy, cyano, methylmercapto or methylsulfuryl, L and M each represents a link formed by the combination of L and M.
US20100160415 Compositions and methods for treatment of autoimmune disease Disclosed are improved methods for the treatment or prevention of an autoimmune disease comprising administration of a modified self-vector encoding and capable of expressing a self-polypeptide that includes one or more pathogenic epitopes associated with the autoimmune disease. The improved method of the present invention includes the administration to a subject of a modified self-vector or self-vectors comprising a polynucleotide encoding a self-polypeptide. In one aspect, the method includes a modified self-vector that allows for increased expression of the self-polypeptide associated with an autoimmune disease in a host cell relative to the unmodified vector. In another, non-mutually exclusive aspect, the method includes a modified self-vector that allows for a secreted autoantigen associated with an autoimmune disease to be encoded as a non-secreted self-polypeptide.
CN101292997A Pharmaceutical composition for treating empyrosis or gastric ulcer, and preparation method thereof The invention discloses American cockroach extracts and a preparation method thereof and also discloses a drug composite for curing burns and scalds or gastric ulcer and a preparation method thereof. The drug combination is composed of the American cockroach extracts and palmatine; the American cockroach extracts are produced by adopting the methods of refluxing extraction, filtration, concentration, etc., and the drug composite is produced by adopting conventional methods of heating dissolution, filtration, etc., simultaneously, the invention also provides a quality control method for the determination of the content of the drug composite; a large number of tests are proved that the method has good efficacy for the treatment of burns, scalds or gastric ulcers, and the clinical use is safe and effective.
US20110097261 Amigo-2-inhibitors for treating, diagnosing or detecting cancer The invention provides, inter alia, methods for treating cancer, compositions for treating cancer, and methods and compositions for diagnosing and/or detecting cancer. In particular, the present invention provides compositions and methods for treating, diagnosing and detecting cancers associated with AMIGO-2 overexpression.
US7132414 Pharmaceutical compositions containing 3-aminoazetidine derivatives, novel derivatives and their preparation The present invention relates to pharmaceutical compositions containing, as active ingredient, a compound of formula: in which R1 represents a radical —NHCOR4 or —N(R5)—Y—R6, Y is CO or SO2, R4 represents a radical -alk-SO2—R11, -alk-SO2—CH═CH—R11 or Het substituted with —SO2—R11 or a phenyl radical substituted with —SO2—R11 or -alk-SO2—R11, R5 represents a hydrogen atom or an alkyl radical, R6 represents a phenylalkyl, Het or Ar radical, to the novel derivatives of formula (I) and to their preparation, as well s to their use in treating various disorders of the nervous system.
WO2005027938A1 Chemotherapeutic antineoplastic treatment Chemotherapeutic antineoplastic method comprising administration of an effective amount of an antineoplastic agent in conjunction with an effective amount of a β-1,3 glucan such as cyclophosphamide and laminarin.
US7071314 Reacting with bromobenzene in presence of palladium catalyst, free of phosphine compound An efficient arylation technique for use in the synthesis of erythromycin derivatives, involving a modified Heck reaction which employs less than six mole percent of palladium catalyst and no phosphine is disclosed. With this modified Heck reaction, an O-alkenylaryl macrolide can be obtained in a much shorter reaction time than under conventional Heck reaction conditions. The modified Heck reaction can be utilized in a method for phosphine-free arylation of an O-allylic erythromycin derivative, in a method for preparing an O-alkenylaryl erythromycin A derivative, or in a method for preparing a 2′, 4″-hydroxyl protected 6-O-alkenylaryl erythromycin A derivative.
US7598254 Substituted 1,3-thiazolo[5,4-d]pyrimidines as xanthine oxidase inhibitors The invention relates to compounds of the following formula (I) or their salts: in which R1 is a group of phenyl, naphthyl, pyridyl or the like which may have a substituent such as an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkoxycarbonyl group having 2-8 carbon atoms, carboxyl, halogen, hydroxyl, nitro, or cyano; R2 is cyano, nitro, or the like; R3 is hydroxyl or the like; X is oxygen, sulfur, or the like; and Y is oxygen or sulfur, and a xanthine oxidase inhibitor containing the compound.
US20090149454 7-((6,7-bis(methyloxy)-4-quinolinyl)oxy)-N-(5 -methyl-3-isoxazolyl)-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide; for prophylaxis and treatment of diseases, such as VEGF mediated diseases; cancer Selected benzomorpholine compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
CN103340904A Composition for treating osteoarthritis The invention provides a composition for treating osteoarthritis and in particular provides a composition, reagent composition or a kit used for treating osteoarthritis and a preparation prepared from the composition, reagent composition or kit product. The composition, reagent composition or kit product is prepared from plasma which contains no red blood cell or white blood cell and is rich in blood platelet and a multifunctional cell component containing fat while other components are combined, and the composition, reagent composition or kit product has the characteristics of quick effect, good treatment effect and low dosage.
US20090169485 Gene therapy and pharmaceutical composition for prevention and treatment of lung cancer Disclosed herein is a gene therapeutic agent and pharmaceutical composition for the prevention and treatment of lung cancer. For aerosol delivery, chemically synthesized polyester amine is used as a carrier in the gene therapeutic agent. The polyester amine/Akt1 siRNA complex is found to be effectively delivered to the lungs of K-ras null mice through a nose-only inhalation system and to significantly suppress lung cancer progression as denoted by gene delivery efficiency and inhibition of Akt-related signals and cell cycle. Thus, the aerosol delivery of polyester amine-mediated Akt1 siRNA is provided as an effective model for noninvasive gene therapy.
CN1606982A Fluconazole formulation Said invention relates to fluconazole contained 2mg-10g/ramal powder injection and frozen-dried powder injection for treating concealed coccus meningitis, pneumonia, general monilial infection (candidemia, monilial peritonitis, monilial endocarditis, monilial pneumonia, monilial urinary tract infection etc), mucous membrane monilial infection (oropharynx, esophagus, skin mucous membrane etc), acute or relapse vagina monilial infection, etc. It also can be use for preventing the mycotic infection inchemotherapy and radiotherapy.
EP1402894B1 Cancerous metastasis inhibitors containing carbacyclic phosphatidic acid derivatives The invention aims at providing novel cancerous metastasis inhibitors by examining carbacyclic phosphatidic acid derivatives for inhibitory activity against the infiltration of cancer cells. The invention provides cancerous metastasis inhibitors containing as the active ingredient compounds represented by the general formula (I): (I) wherein R is linear or branched C1−30 alkyl, linear or branched C2−30 alkenyl, or linear or branched C2−30 alkynyl, with the proviso that each group may contain a cycloalkane ring or an aromatic ring; and M is hydrogen or a counter cation.
CN103202802A In-situ gel formulation for florfenicol injection and preparation method thereof The invention belongs to the field of pharmaceutical formulations specially used for animals, and relates to an in-situ gel formulation for florfenicol injection and a preparation method thereof. The in-situ gel formulation is prepared from antibacterial drugs, an in-situ gel substratum and other indispensable auxiliary materials, wherein the antibacterial drugs are specially used for animals; the in-situ gel substratum is accredited in the field. The preparation method is illustrated.The in-situ gel formulation disclosed by the invention is freely flowing liquid at room temperature, forms the semisolid gel after intramuscular injection or hypodermic injection administration, realizes only one-time administration within one treatment course, has the advantages of easiness for preparation, stability in property, convenience for administration, long administration effect lasting time, definite treatment effect, high animal adaptability, no toxic or side effect or adverse reaction, and the like, achieves the broad-spectrum antibacterial effect and is suitable for preventing and treating various sensitive bacteria infection of the animals, such as pigs, sheep, dogs, cats, cattle, and the like.
US6916847 Anticoagulants; thrombosis; cardiovascular disorders The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
CN102600001A Slow-release mifepristone vaginal ring preparation and application thereof The invention relates to a preparation method for two types of slow-release mifepristone vaginal ring preparations. The first type of slow-release mifepristone vaginal ring preparation includes from 1.0 to 4.5 wt% of mifepristone, from 1.5 to 13.5 wt% of drug scattered carrier, from 0.05 to 20 wt% of surfactant and from 62 to 97.45wt% of medical high polymer release control materials. The second type of slow-release mifepristone vaginal ring preparation includes from 1.0 to 4.5 wt% of mifepristone, from 1.5 to 13.5 wt% of drug scattered carrier, from 0.05 to 20 wt% of surfactant, from 62 to 97.45wt% of medical high polymer release control materials, and a thin release control membrane covered on the outside of each slow-release mifepristone vaginal ring preparation. Due to the preparation method, a slow-release mifepristone vaginal ring can slowly release the mifepristone within seven days, a first pass effect and gastrointestinal reaction of mifepristone orally taken drug are avoided, bioavailability of the drug and pharmacy compliance of a patient are improved.
CN101081232B Yak bone marrow glair polypeptides bone extract and the composition thereof and the preparing method The present invention relates to one kind of yak bone marrow protein polypeptide osseine comprising protein total nitrogen 13-15.8 wt%, free amino acid accounting in nitrogen 1-3 wt%, calcium 0.1-1 wt%, and total phosphorus 0.01-0.1 wt%. The yak bone marrow protein polypeptide osseine contains protein over 80 wt% and various kinds of polypeptide and amino acid. It has simple preparation process and low cost. It may be prepared into composition via adding plant additive and the composition has improved taste, hydroscopicity and flowability. The present invention can provide human body with protein, polypeptides and amino acids.
US7815937 Liquiflash particles and an excipient mass; friability of less than 1%; need for conventional super disintegrant and having a friability of less than 1%; no need for conventional superdisintegrant The invention provides a composition useful for making oral dosage forms capable of dissolving in the mouth in less than 40 seconds without the need for a conventional super disintegrant and having a friability of less than 1%; wherein the composition includes liquiflash particles and an excipient mass. A preferred excipient mass according to the invention contains a directly compressible inorganic salt; a cellulose derivative or a combination of a directly compressible inorganic salt and a cellulose derivative. Preferably, the liquiflash particles and the excipient mass are combined in proportions such that the active ingredient remains substantially within the microspheres when the composition is compressed to obtain a dosage form having a hardness of 20 to 50 N. The compositions of the invention allow for the fabrication of oral dosages having improved hardness and friability.
US20050053553 Combined doses of formoterol and fluticasone The present invention discloses a method and pharmaceutical dry powder combined doses for administration by inhalation of metered dry powder combined doses of finely divided dry medication doses. Formoterol and fluticasone are selected medicaments for forming the combined doses. Metered dry powder medicinal combined doses comprising separately metered deposits of medicinally effective quantities of each of the selected medicaments are prepared, in which the sum of the metered deposits constitutes the metered quantities of powder of the combined doses and the medicinal combined doses are introduced into an adapted inhaler device for a generally simultaneous or sequential prolonged delivery of the medicinal combined doses during the course of a single inhalation by a user, such that each one of the administered medicinal combined doses is composed of a high proportion of de-aggregated fine particles of the selected medicament or medicaments and directed to a selected location in the lungs.
CN101683354A Liver damage relevant drug target and application thereof The invention relates to a liver damage relevant drug target and application thereof. The drug target is stearoyl coenzyme A desaturase (Scd1), and liver damage of mammals can be obviously relieved bydescending the expression of Scd1. The invention also discloses application of antagonist of Scd1 in preparing a composite for inhibiting liver damage of mammals. The invention further discloses a method for screening a potential material for inhibiting liver damage of mammals.
US20100197785 Omega-3 fatty acid fortified composition The present invention relates to an omega-3 fortified composition, method for its production and use of said composition as a nutritional, food or pharmaceutical composition.
CN1824053A Medicine and food dual purpose product for preventing pseudomyopia and true myopia and its manufacturing method A medical product used as both medicine and food for preventing and treating the pseudomyopia and myopia caused by is prepared from composite medicine, vitamins and trace elements. Its preparing process is also disclosed.
CN101204375B Strontium ranelate dry suspension The invention discloses a dry suspension containing strontium ranelate. The dry suspension contains the following components by weight ratio: 50-90 per cent of lactose, or xylitol, or mannite or 50-90 per cent of the combination of lactose, xylitol, mannite; 10-49 per cent of strontium ranelate; 0.1-10 per cent of correctives; 0.1-10 per cent of colorant; and 1-20 per cent of adhesive. With good stability, the dry suspension containing strontium ranelate disclosed in the invention is used for curing and preventing the menopausal osteoporosis.
CN101152463A Externally used medicine liqueur for treating synovitis The present invention discloses an externally applied medicinal wine used for curing synovitis; the raw materials are 170 portion to 190 portion of raw giant typhomium tuber, 290 portion to 310 portion of raw bile arisaema, 290 portion to 310 portion of unprocessed tuber of Pinellia ternate, 290 portion to 310 portion of ledeboruiella roots, 290 portion to 310 portion of tall gastrodia tuber, 290 portion to 310 portion of angelica roots, 290 portion to 310 portion of notopterygium roots, 90 portion to 110 portion of scorpion, 90 portion to 110 portion of centipedes and distilled spirit; the raw materials are ground into fine powder and the medicine powder and the distilled spirit are mixed according to the ratio of 1 to 10 and then the mixture is put in a medicine bottle and sealed for 5 to 8 days to get the finished product of medicinal wine. The present invention adopts the guidance principle of dispelling wind and relieving convulsion, removing sputum and drinking desire and guiding evil out and takes raw giant typhomium tuber and raw bile arisaema as the main ingredients for dispelling wind and removing sputum, relieving convulsion and alleviating pain; other medicines are added for evacuating wind evil and removing sputum and drinking desire to guide the wind evil out; the medicine powder is soaked in the distilled spirit to get the extract; because the medicinal wine liquor is easy to filter into the affected part to remove the disease evil; in this way, the evil is removed and the body becomes healthy and the disease is cured.
US20120122877 Compositions for Treating Bacterial Infections The present invention is antibiotic compositions having the ability to disrupt a MazEF complex in S. aureus. The compositions also have the ability to inhibit growth of S. aureus and as such are useful as antibiotic compounds.
WO2005014576A8 Isoquinolinone derivative, process for producing the same and use thereof A compound of the formula: (wherein the reference marks are as defined in the description), or a salt thereof. There is provided a preventive/therapeutic agent for JNK-associated pathological condition or disorder that exhibits excellent JNK-specific inhibitory activity and excellent oral absorption.
CN102846737A Burn and scald wound treatment spray The invention discloses a burn and scald wound treatment spray. The burn and scald wound treatment spray is characterized in that raw materials comprise 35 parts by weight of mint, 30 parts by weight of poria cocos, 50 parts by weight of red paeony root, 30 parts by weight of siberian elm bark, 25 parts by weight of poppy capsule, 35 parts by weight of borax and 1000 parts by weight of alcohol. A preparation method of the burn and scald wound treatment spray comprises the following steps of crushing mint, poria cocos, red paeony root, siberian elm bark, poppy capsule and borax into crude powder according to the weight part ratio, immersing the crude powder in alcohol for 7 days, filtering to remove dregs and to obtain a soup, and filling the soup respectively into small spray bottles. The burn and scald wound treatment spray has effects of relieving a fever and a pain, inhibiting bacteria and eliminating swelling, and cooling blood and removing stasis, can be used for treatment on burn and scald wounds, and has effects of fast relieving a pain, diminishing inflammation, and preventing and treating wound deterioration infection.
CA2255951C Substituted 3,5-diphenyl-1,2,4-triazoles and their use as pharmaceutical metal chelators 3,5-biphenyl-1,2,4-triazoles of formula (I) have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of an iron overload in the body of warm-blooded animals. Certain of these compounds are novel.
WO2011008230A2 Rapamycin derivatives and ethers of n-propanolamines and uses related to infection The present invention relates to the use of rapamycin derivatives and ethers of N- propanolamines for decreasing infection by a pathogen. More particularly, the invention relates to the use of O-alkylated rapamycin derivatives, as well as bepridil, for decreasing viral infection.
WO2007062076A3 Dexrazoxane formulations and methods Improved formulations of dexrazoxane for making injectable solutions in a clinical setting are provided. In some embodiments, high pH formulations are provided to reduce or eliminate pain upon injection. According to various embodiments, dexrazoxane may be formulated as a lyophilized or non-lyophilized acid salt or as a lyophilized or non-lyophilized free base. In some embodiments, dexrazoxane is provided as a sterile dry milled powder of a free base or an isolated acid salt crystal. Formulations that require significantly reduced clinical preparation time are provided. Single-container presentations of unit doses of dexrazoxane are also provided. The formulations of the present invention may be provided in a vial, infusion bottle or infusion bag. In some embodiments, the container may be directly attachable to a diluent-containing container for easy preparation. In other embodiments, diluent may be added directly to the container. Improved methods of manufacturing dexrazoxane that allow greater processing latitude are also provided.
US20090317372 Small molecules for the reduction of high blood glucose level Embodiments of the present invention include the in vivo use of a family of heterocyclic compounds containing a quaternary ammonium group as exemplified by the thioxanthone and thioxanthene compounds [3-(3,4-dimethyl-9-oxo-9H-thioxanthen-2-yloxy)-2-hydroxypropyl]trimethylammonium chloride, or CCcompound1, N,N,-diethyl-N-methyl-2-[9-oxo-9H-thioxanthen-2-yl)methoxy]ethanaminium iodide, or CCcompound3, and N,N,N-trimethyl-3-(9H-thioxanthen-9-ylidene)-propane-1-aminium iodide, or CCcompound19 to reduce higher than normal blood glucose level within or close to the normal range in subjects with insulin resistance, hyperglycemia, and diabetes thereby also reducing or preventing associated diseases, complications, and pathological states.
CN103068391A Morpholino pyrimidines and their use in therapy There is provided pyrimidinyl compounds of Formula (I), wherein R2 is (1) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
CN102327283A Drug for external use for deodorization and perspiration absorption The invention discloses a drug for external use for deodorization and perspiration absorption, which is made into a pulvis or a spraying agent according to the different characteristics of the drug for the external use by using talcum powder and nano zinc oxide as raw materials. The drug for the external use for the deodorization and the perspiration absorption is convenient to use and simple to prepare, does not appear desquamation and furfuration phenomena in a treatment process, further has a quite good curative effect, does not have any side effects, and further has cheap price.
CN103169668A Painless synergistic amoxicillin powder injection for animals and preparation method thereof The invention belongs to the field of the medicines for animals and discloses a painless synergistic amoxicillin powder injection for animals and a preparation method thereof. The powder injection comprises the following components in parts by weight: 48-52 parts of amoxicillin or amoxicillin sodium (active ingredient), 10-30 parts of a cosolvent, 1-3 parts of an analgetic, 5-8 parts of probenecid sodium and 1-2 parts of an antifebrile anti-inflammatory analgesic. The preparation method of the powder injection comprises the following steps of: in parts by weight, evenly mixing 1-3 parts of analgetic, 5-8 parts of probenecid sodium and 1-2 parts of antifebrile anti-inflammatory analgesic together, and then evenly mixing the mixture with 48-52 parts of amoxicillin or amoxicillin sodium (active ingredient) and 10-30 parts of cosolvent, thereby obtaining the painless synergistic amoxicillin powder injection. The amoxicillin powder injection prepared by the preparation method provided by the invention solves the problems of strong injection pricking stress, poor effects of anti-inflammation and analgesia, and heat elimination and defervescence, ingestion reduction after the administration of the drug, and the like; and the product is highly required in clinical application, and is wide in market prospect and huge in social benefit.
US20100113383 Bifidobacterial gene sequences and their use This invention provides nucleic acids and proteins involved in oligosaccharide modification in the species Bifidobacteria. The invention provides methods for utilizing the proteins of the invention to generate human milk oligosaccharides or oligosaccharide mimics. The invention also provides compositions containing the human milk oligosaccharides or oligosaccharide mimics and methods for use.
CN101804066A Application of MPEG-PLA (Methoxypolyethylene Glycols-Polylactic Acid) diblock copolymers in preparation of medical anti-blocking material The invention relates to the field of medical high polymer materials, in particular to an application of MPEG-PLA (Methoxypolyethylene Glycols-Polylactic Acid) diblock copolymers in preparation of medical anti-blocking materials. The invention aims at providing a new selection for the medical anti-blocking material. The technical scheme for the technical problem is to provide the application of MPEG-PLA diblock copolymers in preparation of medical anti-blocking materials. The molecular weight of the MPEG-PLA copolymer is 3,000-12,000, wherein the ratio of the molecular weight of a PEG (Polyethylene Glycol) chain segment to the molecular weight of a PLA (Polylactic Acid) chain segment is 0.8-2, the copolymer can be dissolved in water to form a solution and can also form gel under certain conditions. The experimental result shows that the MPEG-PLA block copolymer hydrogel can be applied to medical anti-blocking materials with multiple excellent characteristics and provides a new selection for the field needing the medical anti-blocking materials.
WO2014117274A1 Imidazopyridine compounds and uses thereof This invention generally relates to substituted imidazopyridine compounds, particularly substituted 4-(imidazo[1,2-a]pyridin-2-yl)benzamide compounds and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.
US7872011 Inhibition of phosphoinositide 3-kinase β The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase β, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory activity of PI 3-kinase β of the compound. The invention also relates to novel compounds that are inhibitors of PI 3-kinase.
US7615657 Method of producing an oil extract from seeds of plants via a binary azeotropic solvent mixture The invention describes a method of producing extracts from the seeds of meadowfoam, brassicas and crambe plants. A number of subsidiary processes and steps are shown in order to extract differing fractions of oil. Products produced from the above method are also described including uses and methods of these products which include a variety of skin conditions including eczema, facial eczema, dermatitis, external ulcers, welts, rashes, insect bites, allergic reactions and other irritations, burns, wounds, psoriasis, acneiform eruptions, dryness, dry skin, irritation, skin atrophy, secondary infections and the like. The extracts are also described as being a useful compound for treatment of the symptoms of such skin conditions as described above. In particular the use and extraction of glucosinolate (GSL), thiocyanates (TCL) and isothiocyanates (ITCL) is described.
WO2008071173A1 Preparations for inhibiting prostaglandin e2 synthesis The present invention relates to preparations of acylphloroglucinols, in particular hyperforin and myrtucommulone and derivatives thereof, the provision of these preparations for the therapeutic treatment of inflammatory diseases, painful and feverous conditions and cancer diseases which are accompanied by increased activity of the inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) or increased prostaglandin E2 synthesis, and also the appertaining methods.
CN103211752A Preparation and application of in-situ gel used for nystatin pH sensitive type vagina The invention relates to the medicine technical field, and is a novel dosage form of nystatin, and a preparation and an application of an in-situ gel used for nystatin pH sensitive type vagina. The in-situ gel is characterized in that the preparation is a solution at an unphysiological state, can be the gel at a physiological state, wherein the nystatin pH sensitive in-situ gel is prepared by employing carbomer 980 and poloxamer F127 with a proper ratio. The viscosity of the preparation is less than 1100mpa.s at the unphysiological state and the viscosity of the preparation is greater than 2500mpa.s at the physiological state when the pH value is greater than 4.5. The preparation prolongs the detention time of nystatin in vagina, the curative effect is increased, and the preparation has good application prospect.
US6979689 Antitussive, decongestant and diphenhydramine antihistamine; cough, congestion and allergy symptom relief A composition of an antitussive, a decongestant, and diphenhydramine as an antihistamine to treat upper respiratory and oral pharyngeal congestion and related symptoms in a patient. In addition to providing antihistamine effects, diphenhydramine also provides effects as an anti-cholinergic, an analgesic, an antitussive, and an analgesic adjuvant.
WO2009073885A1 Leukemic stem cell ablation A method for treating a leukemia patient that is resistant to a thymidine kinase inhibitor (TKI) other than imantinib comprising administering a cephalotaxine to said patient until said patient demonstrates a hematological or cytological response to said leukemia.
WO2012167457A1 Use of hypericum japonicum thunb. general flavone in preparing medicament for treating hepatic fibrosis The use of hypericum japonicum Thunb. general flavone in preparing medicament for treating hepatic fibrosis is provided in the present invention. The hypericum japonicum Thunb. general flavone is an effective component extracted from hypericum japonicum Thunb.. A medicinal composition for treating hepatic fibrosis, which comprises the hypericum japonicum Thunb. general flavone and pharmaceutically acceptable carrier is also provided in the present invention.
WO2010046273A2 Pyrimidinyl pyridone inhibitors of jnk This application discloses novel pyrimidinyl pyridone derivatives according to Formulae I and II, wherein R1 and R2 are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of Formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of Formula I to a subject in need thereof.
WO2006102079A1 N- [3- (1-amin0-5, 6, 7, 8-tetrahydro-2 , 4, 4b-triazafluoren-9-yl)-phenyl] benzamides as tyrosine/threonine kinase inhibitors, in particular b-raf kinase The present invention relates to compounds that are useful to inhibit, regulate and/or modulate tyrosine and serine/threonine kinase and kinase-like proteins, such as RAF kinase, a serine/threonine kinase that functions in the MAP kinase signaling pathway. The application is also concerned with compositions which contain these compounds, and methods of using them to treat tyrosine and serine/threonine kinase and kinase-like dependent diseases, such as angiogenesis, cancer and cardiac hypertrophy, and with other subject matter.
WO2008019284A1 Phenoxymethylalkyne inhibitors of lta4h for treating inflammation A chemical genus of biphenyl heterocycle derivative inhibitors of LTA4H (leukotriene A4 hydrolase) of the formula: is disclosed, hi these compounds Q and Z are (CH2)1.10; in which one or two (CH2) may optionally be replaced by -O-, -NR1-, -SO-, -S(O)2-, -C(=O)- or -C=O(NH)-; Het is a 5-7 membered non-aromatic nitrogen heterocycle; and W is acyl, hydroxyl, carboxyl, amino, carboxamido, aminoacyl, -COOalkyl, -CHO, heterocyclyl, substituted aryl, or substituted heterocyclyl, or taken together ZW can be H or -COOalkyl. The compounds are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
CN103446115A Applications of Sarcaboside A in medicament against human fungus The invention relates to applications of Sarcaboside A in preparing a medicament against human fungus, and belongs to the field of medicines. The Sarcaboside A plays a strong role in inhibiting trichophyton rubrum, microsporum lanosum or trichophyton tonsurans, therefore, the Sarcaboside A can serve as a compound with an anti-human fungus function, and is expected to be applied in preparing related medicaments. The applications of the Sarcaboside A in preparing the medicament against human fungus are disclosed for the first time. As a skeleton type of the Sarcaboside A belongs to a brand-new skeleton type, the Sarcaboside A has an unexpectedly strong human fungus inhibition activity, and the possibility of giving any inspiration by other compounds does not exist. The Sarcaboside A has significantly substantive characteristics, as well as obviously prominent progress in the prevention and treatment of the human fungus infection.
CN102319211A Preparation process and application of tryptanthrin injection emulsion The invention provides a medicament for treating leucocythemia and other tumors, colonitis and fungal infection, namely a tryptanthrin injection emulsion, and a preparation process thereof, and belongs to the fields of pharmaceutical manufacture and clinical application. The tryptanthrin injection emulsion is characterized in that: tryptanthrin has the effects of killing and inhibiting tumor cells, transplanted tumors in animals, various fungi and bacteria, an effect of inhibiting inflammation, as well as regulation and other pharmacological activities to the immunity of a body. The tryptanthrin injection emulsion prepared by the tryptanthrin for treating leucocythemia and other tumors, colonitis and fungal infection can be used for treating the leucocythemia and other tumors, colonitis, fungal infection and other diseases. The tryptanthrin injection emulsion has the advantages of stable medicament, controllable quality, high bioavailability, small administration dosage, exact curative effect, low side response, rich raw material source and low production cost.
CN101194917A Grifola frondosa oral liquid rich in gastrodine, organic selenium and method for preparing the same The invention discloses oral liquid of grey polypore which is rich in gastrodine and organic selenium and a process for preparation. Fresh gastrodia elata and bitter garlic are pre-processed, dried, and grinded by the invention, which take deep fermentation with grey polypore in powder shape to prepare oral solution which is rich in gastrodine, crude polysaccharide, and organic selenium. The process for preparation comprises first, culturing bacterial of a slant face of the grey polypore, second, culturing liquid seed, third, processing raw material which are gastrodia elata and bitter garlic, fourth, fermenting, fifth, post-treating products. In the oral liquid of the invention, the content of gastrodine is 2.2 to 2.8mg/100ml, the content of crude polysaccharide is 4.0 to 4.8mg/L, and the content of organic selenium is 0.11*10-6 to 0.21*10-6. Compared with the prior art, the oral liquid of the invention can play a stronger effect of anti-tumor and enhance human immunity, and inhibit and kill cancer cells without hurting normal cells of human bodies simultaneously, which can service for human health. The process of the invention can lead gastrodine, bitter garlic, and grey polypore to be fermented together to prepare oral solution which is rich in gastrodine, crude polysaccharide, and organic selenium, and the oral solution can be produced in large scale.
US20080200451 Antitumor agents; use in combination with other drugs such as pentamidine Compounds of the formula (I), in which W, R, R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.
WO2013106175A1 Variant activin receptor polypeptides, alone or in combination with chemotherapy, and uses thereof The present invention provides variant activin IIB soluble receptor polypeptides and proteins capable of binding and inhibiting the activities of activin A, myostatin, or GDF-11. The present invention also provides polynucleotides, vectors and host cells capable of producing the variant polypeptides and proteins. Compositions and methods for treating muscle-wasting and other diseases and disorders are also provided.
WO2007071967A3 Substituted phenol derivatives as analgesics The present invention concerns the use of compounds derived from the anaethetic propofol that are useful as analgesics. The compounds act as activators of glycine receptors and may have greater activity at glycine receptors in the peripheral nervous system than at GABA receptors in the central nervous system.
CN1872108A Drop pills of centella total glycoside, and preparation method A dripping pill of asiaticoside for treating wound features high natural level and safety and low toxic by-effect. Its preparing process is also disclosed.
WO2005063227A1 Process for producing triterpene composition A process for producing a triterpene composition which comprises culturing a callus induced from banaba, loquat, perilla, or guava together with indoleacetic acid and a vegetable hormone other than the acid and obtaining from the cultured callus a triterpene composition which contains at least one member selected from the group consisting of corosolic acid, tormentic acid, 2α,19α-dihydroxy-3-oxours-12-en-28-oic acid, and maslinic acid.
WO2011140817A1 1-[(4-hydroxypridin-4-yl) methyl] pyridine-2(1h)-one derivatives, preparation methods and uses thereof Provided are N-[(4-hydroxypridin-4-yl) methyl] pyridine-2 (1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxy tryptamine 1A receptor agonist and 5-hydroxy tryptamine reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxy tryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.
EP2400988A1 Compositions, use and method for the use of surface active proteins in topical drug delivery across keratin The present invention provides the use of surface active proteins, especially class I and class Il hydrophobins, in topically applied pharmaceutical formulations. The invention is particularly directed to topically applied pharmaceutical products for enhancing the penetration to achieve a transungual delivery of a prophylactically and/or therapeutically effective amount of an active ingredient (drug) to a patient (including animals and humans) into and/or through a nail, of the animal or human body, in order to treat one or more of a variety of diseases or disorders. Related embodiments of the invention are also disclosed.
CN101972271A Chlorine dioxide mucous membrane gel and preparation method thereof The invention discloses a chlorine dioxide mucous membrane gel and a preparation method thereof. Firstly disodium ethylene diaminetetraacetate is dissolved in purified water, thus obtaining disodium ethylene diaminetetraacetate aqueous solution; one half of the disodium ethylene diaminetetraacetate aqueous solution is taken and warmed, hydroxypropyl methyl cellulose is stirred and dispersed into the warmed disodium ethylene diaminetetraacetate aqueous solution, thus obtaining mixed solution, and cooling to room temperature is carried out, thus obtaining clear mixed solution; the rest half of disodium ethylene diaminetetraacetate aqueous solution is mixed and dissolved with medical grade glycerol and carbomer 934P, and sodium hydroxide aqueous solution is dropwise added, thus obtaining gel base material; and then the clear mixed solution, the gel base material and demand-release chlorine dioxide aqueous solution are mixed, stirred and vacuum defoamed, thus obtaining the chlorine dioxide mucous membrane gel. The invention has rapid, durable and reliable disinfection and sterilization effects, can rapidly and thoroughly kill off all the microorganisms in mouth, nasal cavity, vagina and mucus in anus cavity as well as microorganisms on anus cavity mucosa.
US20120076740 Water soluble pharmaceutical compositions of hops resins The present invention is drawn to water-soluble compositions for providing hops constituents, particularly alpha acids, iso-alpha acids, and beta acids. A pharmaceutical gel composition can comprise a hops extract and a surfactant. Such compositions can be formulated into products for various therapeutic applications, including oral and topical uses. Such compositions can also be dissolved in water to yield a clear solution containing more dilute hops acids. The invention also provides methods of treatment comprising administering water-soluble hops compositions. The present invention is also drawn to methods for making water-soluble preparations of hops constituents.
US20080275110 Increased oral absorption and/or transfer into blood circulation; foods, beverages; for lowering blood cholesterol levels Sesamin and episesamin are incorporated at specified weight ratios in oral compositions so that the oral absorption of episesamin and/or its transfer into blood circulation is increased. Sesamin and episesamin are also incorporated at specified weight ratios in oral compositions so that the physiological activities of sesamins are enhanced.
US20100035926 Pyrazole derivatives as non-steroidal glucocorticoid receptor ligands The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation.
US20100160324 Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R1 is an optionally substituted heterocyclic group having from 3 to 12 ring members provided that the cyclic group joined to the pyrazole contains at least one heteroatom selected from N, O or S; A is a bond or —Y—(B)n—; B is C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C1-8 hydrocarbyl group; with the proviso that R1 is not formula (II): where X, R3′ and R4′ are defined in the claims.
WO2006013003A1 Use of products derived from selenoprotein t, in its application related to calcium homeostasis The invention is based on the characterization of selenoprotein T (SelT) as involved in the regulation of intracellular calcium. Therefore, the invention concerns compositions comprising SelT or a polynucleotide capable of expressing or inhibiting the expression of SelT in a host cell. In particular, the invention concerns pharmaceutical compositions for treating diseases related to a calcium homeostasis defect.
WO2006080884A1 Novel biaromatic compounds, inhibitors of the p2x7-receptor The invention provides compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein Ar1 represents a group (II), (III), (IV) or (V), and A, Ar2, n, R1, R2, R3, R4 and R5 are as defined in the specification; a process for their preparation; pharmaceutical compositions containing them; and their use in therapy.
CN1745803A Longxuejie extract with alpha-glycosidase inhibiting activity and its quality control A hypoglycemic extract of Dragon's blood, which has the activity for suppressing alpha-glycosidase, is disclosed. Its quality control method includes the discrimination method (efficient liquid-phase discrimination and thin-layer chromatographic discrimination) and the content measuring method (spectrophotometric method and fluorescent analysis method).
CN102188406A Preparation method of taste-concealing micro-capsules of levofloxacin hydrochloride The invention relates to a preparation method of taste-concealing micro-capsules of levofloxacin hydrochloride. The application of the levofloxacin hydrochloride to treating animal diseases is greatly limited by the bitterness of the levofloxacin hydrochloride. The preparation method of the taste-concealing micro-capsules of the levofloxacin hydrochloride comprises steps of dissolving 5% to 90% of the mixture of acrylic resin II or acrylic resin III or acrylic resin II and acylic resin III with 20% of sodium hydroxide solution to prepare 5% to 10% of wall material solution, adjusting the solution into an alkalescent solution, adding distilled water to dissolve levofloxacin hydrochloride to prepare 10% to 40% of core material solution, mixing the wall material solution and the core material solution, adding 0.5% to 5% of Span 80 to prepare 1-10 times of quality of atoleine, carrying out high-shear emulsification and dispersion to the mixture to prepare a stable WxO emulsion type emulsion, stirring the emulsion, dripping hydrochloric acid into the solution to adjust the solution to an acid solution, dissolving the wall material out to cover the surface of capsule core material, and filtering and drying the surface of the capsule core material, and adding a small amount of magnesium aluminum silicate to absorb the residual atoleine. The invention is applied to medicines.
WO2006068212A1 Lipase inhibitor and preventive/remedy for skin diseases It is intended to provide a lipase inhibitor containing, as the active ingredient, “proanthocyanidin” or “a cranberry extract containing proanthocyanidin”; a preventive/remedy for skin diseases caused by bacterial lipase; and foods, drinks, drugs or cosmetics containing the same.
EP1385502B1 Medicament comprising an anhydrous formulation of xanthogenate The invention relates to anhydrous, pharmaceutical formulations of xanthogenates, to the production thereof and to agents containing said formulations for the treatment of virus, tumor or autoimmune diseases. The pharmaceutical preparations contain a xanthogenate of formula (I), wherein R1 represents an optionally substituted aryl or alkyl radical and R2 represents a metal atom, an optionally substituted alkyl, alkoxy, amino or ammonium group or halogen. Said preparations also contain an emulsifying agent that reduces the irritating effect of the xanthogenate and optionally an adjuvant enhancing the activity of the xanthogenate.
US20110076321 Self-adhesive polymer matrix containing sea algae extract A self-adhesive polymer matrix which comprises a polymer that forms a gel in water, water, a sea algae extract, and a monohydric or polyhydric alcohol.
US8703820 Administration of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid for the treatment of dermatological disorders Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.
CA2214448C Cereal food product high in soluble fiber An extrusion cooked cereal product in ready-to-eat form. The cereal product contains a defatted oat bran concentrate which has a .beta.-glucan content of at least 10 % by weight and in an amount so that the cereal product has a .beta.-glucan content of at least 5 % by weight.The cereal product in solution providing a viscosity at least as great as the viscosity provided by the components of the cereal product prior to being extrusion cooked. The cereal product is useful in the treatment and prophylaxis of diabetes.
CN101015544B Use of phenyl propyl compound with oxidation resistance function for protecting liver and brain damage This invention relates to an application of phenylpropionic acid styracine type and cinnamic acid styracine type curcumin analogs in resisting oxidation, and protecting liver and preventing brain damage. The compound has effects in protecting liver cells of suckling mouse from damage, promoting liver cells repair, scavenging superoxide anion and DPPH in vitro, inhibiting the generating activity of lipid peroxide, protecting pheochromocytoma cell simulating cranial nerve from damaging, and chelating iron ion. Thus it is can be expected to be used for preparing medicine for preventing and treating chronic or acute liver or brain damage diseases, apoplexy, sequelae of apoplexy, Parkinson's disease, senile dementia, inflammation, autoimmune disease, tumour, myocardial ischemia, cardiac hypertrophy, senility, allergic response, and atherosclerosis.
CN101143872B 3-halogen substituted cephalosporin derivative The present invention belonging to the technical field of medicines relates to a new cephalosporin derivative with three sites substituted by halogen, a hydrolyzable ester or a medicinally acceptablesalt of the cephalosporin derivative, a preparation method of the compounds, medicinal composites containing the compounds and the applications of the composites in the preparation of medicines used to cure and / or prevent infectious diseases. Researches show that the new cephalosporin derivative and the hydrolyzable ester or the medicinally acceptable salt of the cephalosporin derivative has theadvantages of broad-spectrum and high-efficiency antibacterial effect, low drug resistance, etc. the invention has excellent clinical value and can be widely used in the clinic.
EP2034991B1 Preparation for preventing ageing symptoms containing phytoestrogens and melatonin The present invention refers to a preparation for preventing the symptoms of ageing in a human body, and a method for maintaining a correct chronobiological mechanism in the body. The preparation comprises a first dosage unit including soy isoflavones with a genistein content of at least 50% and a second dosage unit including melatonin or a precursor thereof and soy isoflavones with a genistein content of at least 50%, wherein the first and the second dosage units are distinct units to be administered separately from each other.
WO2013171224A1 Radioactive rhodium complexes, preparation methods and uses thereof The present invention concerns radioactive rhodium complexes, their preparation methods, and their use for the radiolabelling of biomolecules, especially monoclonal antibodies.
WO2011127333A3 Compounds for treating disease, for administering, and for pharmaceutical compositions Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).
WO2012138013A1 Paclitaxel-loaded polymeric nanoparticle and preparation thereof Provided are paclitaxel-loaded polymeric nanoparticles, including paclitaxel and a water-soluble polymer with which the surface of paclitaxel is surrounded and coated, wherein the polymer is poly[2-(dimethylamino)ethyl methacrylate-co-methacrylic acid (PDM). The paclitaxel-loaded polymeric nanoparticles are those having paclitaxel surrounded with a copolymer, have water solubility and biocompatibility, and release and transport the drug, paclitaxel, to cancer cells having multi-drug resistance (MDR), thereby providing an anti-cancer effect several thousand times higher than the effect of original paclitaxel.
CA2343120C Use of an anthracycline derivative for the treatment of a liver tumor The present invention relates to the use of methoxymorpholino doxorubicin for the treatment of a liver cancer; in particular, it refers to the intrahepatic administration of methoxymorpholino doxorubicin for use in the liver tumor therapy optionally in association with an agent which remains selectively in liver tumor after its injection through the hepatic artery.
US20100173988 Oxaliplatin active substance with a very low content of oxalic acid The present invention relates to an oxaliplatin active substance for a pharmaceutical composition, wherein its weight content in oxalic acid is not more than 0.08%, and to a process of preparing the active substance.
US20090048159 Kit for treating a health condition by inducing translocation of a calreticulin protein to a cellular membrane A kit for treating a health condition in a mammal comprises a calreticulin protein and/or compound for inducing a translocation of a calreticulin protein to a cellular membrane in order to provoke an immunogenic apoptosis. The calreticulin protein may include any one or more of: endogenous calreticulin, recombinant calreticulin, and calreticulin in mimetic form. The endogenous form of calreticulin may include any one of: a plasma membrane calreticulin and an intracellular calreticulin.
US20080107740 Dry powder inhaler; metered dose nebulization; asthma or other inflammatory respiratory disorders; correct molecular ratio of salmeterol active in the lung while budesonide active in the lung can be ensured Pharmaceutical composition for inhalation, containing as active ingredient effective amounts of salmeterol or a physiologically salt of salmeterol or a solvate thereof, and budesonide or a therapeutically salt of budesonide or a solvate thereof, wherein the molecular ratio of salmeterol component to budesonide component is in the range 1:2 to 1:50, together with a pharmaceutically acceptable carrier.
US20090041740 Cancer treatment by metabolic modulations The invention provides compositions and methods for inhibiting the growth or proliferation of hyperproliferative cells or inducing regression of hyperproliferative cells. More specifically, the invention provides compositions and methods for stimulating glycogen accumulation in target cells (e.g., hyperproliferative cells) in order to increase glycogen to a level that is toxic to the target cell.
US20130023589 Medication for therapy or prophylaxis of asthma A medication for therapy or prophylaxis of asthma, comprises a ginger compound selected from a group of [6]-gingerol, [10]-gingerol, [6]-shogaol and [6]-gingerol; and an acceptable carrier or excipient, which can relieve the airway remodeling symptoms of asthma, particularly to phthalate induced airway remodeling, by suppressing the proliferation and migration of bronchial smooth muscle cells and reducing the instances of fatal asthma.
US20120128582 Methods and compositions of [32p]-labeled adenine nucleotides for the treatment of atherosclerosis, vascular arterial diseases and coronary artery diseases A method for the treatment of atherosclerosis. The method includes the administration of a 32P-labeled agent as a beta emitter, such as 32P-labeled ATP or other 32P-labeled adenine nucleotides, whereby the 32P-labeled agent seeks and then permeates the atherosclerotic plaque en bloc without prior degradation. The accumulation of the 32P-labeled agent in the atherosclerotic plaque is achieved at time points whereby the 32P-labeled agent is cleared from the blood. Thus, radionuclide-labeled adenine nucleotides accumulate with high specificity in atherosclerotic lesions and in the heart. The beta particles (electrons) emitted by the 32P-label have a maximal path distance of about 0.5 cm and their energy preferentially destroy cells present in the atherosclerotic plaque without affecting vessel integrity or inducing arterial thrombosis.
CN101836995A Compound sulfamonomethoxine sodium multivesicular liposome and preparation method thereof The invention discloses a compound sulfamonomethoxine sodium multivesicular liposome and a preparation method thereof. The compound sulfamonomethoxine sodium multivesicular liposome is prepared from lipid, sulfamonomethoxine sodium as a hydrophilic medicament and trimethoprim as a lipophilic medicament, wherein the sulfamonomethoxine sodium and the trimethoprim are simultaneously packaged in the multivesicular liposome structure formed from soya bean lecithin, cholesterol and triacylglycerol; when the multivesicular liposome is synthesized, the addition ratio of the total mass of the sulfamonomethoxine sodium and the trimethoprim to the total mass of lipid is preferably 1:4; the added mass ratio of the sulfamonomethoxine sodium to the triacylglycerol is preferably 4:1; the added mass ratio of the soya bean lecithin to the cholesterol is prefertably 1:1; and the use level of the triacylglycerol is preferably 16/mmol*L-1. During preparation, the ratio of the first emulsification time to the second emulsification time is preferably 4:1 (12 min:3 min). In the liposome, two medicaments with different dissolving characteristics of water solubility and lipid solubility are mixed together to be applied to the same multivesicular liposome; and the multivesicular liposome has the advantages of long slow releasing time, high packaging rate, good stability, can be used as a new preparation of veterinary medicine and lays foundations for clinical generalization and application.
WO2013187462A1 Piperidinylpyrazolopyridine derivative A compound represented by general formula (I) [wherein R represents an aryl group which may be substituted or a heteroaryl group which may be substituted] or a pharmacologically acceptable salt thereof, which has an excellent LCAT activation activity and is useful as an active ingredient for a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart diseases, coronary heart diseases (including heart failure, cardiac infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance and angiogenic restenosis), cerebrovascular diseases (including stroke and cerebral infarction), peripheral vascular diseases (including diabetic vascular complications), dyslipidemia, low-HDL cholesteremia, or renal diseases, particularly an active ingredient for an anti-arteriosclerosis agent.
CN101016557A Muskrat fragrant active component prepared by external secretion, preparing process and use The invention discloses a preparing method of muskrat fragrant active component with external secret scent, which comprises the following steps: supplying naphthene ketones with 7-21 carbon, fatty acid and ester, naphthenic alcohols with 3-33 carbon, aldehydes and alkenes; stripping fragrant gland bag of muskrat; shearing cortex part; washing with PBS; adding into original generation culture liquid; producing suspended liquid; feeding on the floor of culture bottle; adding into culture liquid to culture; choosing cell of fine and close step; adding into parenzyme; digesting; blowing cell single-layer slowly; sucking-off; transferring into another culture bottle; adding into culture liquid; culturing at constant temperature; extracting out of muskrat aromatic oil state matter; adding into parenzyme; reacting; adding into 1, 3 methyl glycol or dimethy ketone; stewing; separating; adding into kalii permangana; stewing with activated char; removing the kalii permangana; centrifuging; extracting with 1, 3 methyl glycol; removing solvent. This preparing craft is simple and stable, which is a new animal spice and medicinal material.
WO2010007034A1 Use of pyrimidylaminobenzamide derivatives for the treatment of fibrosis The invention relates to the use of a pyrimidylaminobenzamides of formula (I) wherein the radicals have the meanings as defined herein,or of a pharmaceutically acceptable salt thereof for the manufacture of pharmaceutical compositions for use in the treatment of fibrosis, to the use of a pyrimidylaminobenzamides of formula (I) or pharmaceutically acceptable salt thereof in the treatment of fibrosis, to a method of treating warm-blooded animals including humans suffering from fibrosis by administering to a said animal in need of such treatment an effective dose of a pyrimidyl- aminobenzamide of formula I or a pharmaceutically acceptable salt thereof, and to combinationscomprising(a) at least one pyrimidylaminobenzamides of formula (I) as and (b) at least one compound selected form AT1-receptor antagonists and ACE inhibitors and the use of such combinations in the treatment of fibrosis, in particular hepatic fibrosis.
CN101304747A Combinations comprising a VEGF receptor inhibitor and a penetration enhancer The present invention relates to a composition comprising a VEGF receptor inhibitor and a penetration enhancer and uses thereof , for the treatment of dermatological diseases selected from psoriasis, atopic dermatitis and acne.
CN101756889A Lamivudine ester injection and preparation method thereof The invention discloses a lamivudine ester injection and preparation method thereof. The injection consists of lamivudine ester, non-aqueous solvent, cosolvent and water for injection, wherein the weight-volume ratio (g/ml) of the lamivudine ester to the non-aqueous solvent is 1:10-100, preferably 1:15-60; the proportion of the dosage of the non-aqueous solvent in a prescription is 20 to 60 percent (v/v); the dosage of the cosolvent is 1 to 20 percent (w/v); and injection contains 0.5 or 1.0 g/ml of lamivudine ester. Accelerated stability test, animal hemolysis test, heat source examination, irritation test and allergy test verify that the lamivudine ester injection completely meets provisions and standards. The injection has the characteristics of stable quality, quick response and low toxic/side effect, avoids solution turbidness, incapable administration and other problems when the injection is diluted in clinical use, and can meet clinical need.
EP2235018A1 Pharmaceutically acceptable salts of methyl (3-{ ýý3-(6- amino- 2-butoxy-8-oxo-7, 8-dihydro-9h-purin-9-yl) propyl¨(3- morpholin-4-ylpropyl) amino¨methyl }phenyl) acetate and their use in therapy The present invention concerns hydrochloric acid, hydrobromic acid and maleic acid salts of methyl (3-{ [ [3- (6-amino-2- butoxy-8-oxo-7, 8-dihydro-9H-purin-9-yl) propyl] (3-morpholin-4- ylpropyl) amino] methyl} phenyl) acetate, compositions comprising them and their use in therapy.
US20100280014 N-phenyl- (piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein X is a bond or a group N—R4; R1 is hydrogen or methyl; R2 is hydrogen or methyl; R3 is hydrogen, C1-C3 alkyl, fluorine, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, or C3-C4 cycloalkyl-CH2—; R5 is hydrogen, fluorine, chlorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R6 is hydrogen, fluorine or chlorine; and n is 1 or 2.
US20080188448 reduced antiglucocorticoid effects; side effect reduction; endometriosis, leiomyomas of the uterus, dysfunctional bleeding, dysmenorrhoea; antitumor agents; female fertility control, for hormone replacement therapy; 6-[2(2,2-Dimethylpropyl)-2-hydroxypent-3-ynoylamino]-4-methyl-2,3-benzoxazin-1-one The present invention relates to non-steroidal progesterone receptor modulators of the general formula I, the use of the progesterone receptor modulators for the manufacture of medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.
CN1969816A Anticancer sustained release agent containing epothilone Disclosed is an anti-cancer drugs slow release agent containing Epothilone which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents include Epothilone, Epothilone derivatives, Epothilone B, Epothilone D and combination of anti-cancer drugs selected from phosphoinositide-3-kinase inhibitor, of pyrimidine analogues and/or DNA restoring enzyme inhibitor, the slow release auxiliary materials include polylactic acid and its copolymer, polyethylene glycol, PLA-COOH copolymer, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid), Polifeprosan, polylactic acid and other biocompatible high polymers, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose. The anticancer active constituents and the slow release microspheres can also be prepared into slow release implanting agent for intra-tumor or around-tumor injection or placement for the effective suppression of tumor growth and for the appreciable enhancement for curative effects of non-operative treatments such as chemotherapy.
WO2013132428A1 Therapeutic preparation and process for preparing said therapeutic preparation A therapeutic preparation (1) comprising ozonised oil and a platelet concentrate (2), mixed according to a mixing ratio between the volumes of the platelet concentrate (2) and of the ozonised oil (3) substantially in the range between 2 and 4.
WO2010143719A1 Alkaline decomposition product of hop extract and use thereof A food and a food additive, each of which comprises an alkaline decomposition product of a hop extract; and a fat accumulation inhibitor or an agent for inhibiting the increase in body weight, which comprises the alkaline decomposition product as an active ingredient.
US20090022709 Control of sorbose utilization genes and uses thereof This invention relates generally to the discovery of a novel control of sorbose utilization (CSU) genes. The invention further relates to the detection of these genes and their use in the diagnosis and treatment of fungal infections.
US20100076087 Methods of reduction of interpatient variability Disclosed herein are methods for the reduction of inter-patient variability of a drug, such as in one or more parameters including half-life (t1/2), maximum plasma concentration (Cmax), time at maximal plasma concentration (Tmax), area under the time-versus-concentration curve (AUC). Also provided are methods of reducing side effects associated with drugs.
CN102552273A Composition containing epigallocatechin gallate and methotrexate The invention belongs to the fields of medicine and gene engineering, and provides a composition for suppressing tumor cell proliferation. The composition for suppressing tumor cell proliferation comprises epigallocatechin gallate and methotrexate serving as active ingredients, and pharmaceutically-necessary auxiliary materials, wherein the molar ratio of the epigallocatechin gallate to themethotrexate is 800:3-1.5:1. As proved by experiments, the treatment effect of methotrexate on the suppression of tumor cell proliferation can be enhanced remarkably by using the composition prepared from the epigallocatechin gallate and the methotrexate or using the epigallocatechin gallate during dosing of the methotrexate. The composition basically has no toxicity on the liver and kidney of a nude mouse, the epigallocatechin gallate in the active ingredients has rich resources and low price, and the treatment cost of a tumor patient is reduced while the tumor suppression rate is increased simultaneously.
WO2011009061A1 Compositions comprising a cholinesterase inhibitor for treating cognitive disorders Disclosed herein is a pharmaceutical composition comprising a cholinesterase inhibitor and compound of the following formula: The composition is effective for treating cognitive disorders, and methods of treating such disorders using the composition are also disclosed.
WO2008104077A1 Small molecule inhibitors of protein arginine methyltransferases (prmts) The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as defined herein. Said compound are useful as inhibitors of PRMTs and/or CARM-I. The invention further relates to compositions comprising such compounds and methods for their use.
CN103251605A Application of Myriberine A in preparing medicine for treating breast cancer The invention discloses an application of Myriberine A in preparing a medicine for treating breast cancer, belonging to the technical field of a new application of a medicine. According to in-vitro MTT anti-tumor activity evaluation, the Myriberine A also has an obvious inhibition effect on the growth of human breast cancer cell lines 4T1, MCF-7, MDA-MB-231 and MCF-7B. Therefore, the Myriberine A can be used for preparing an anti-breast cancer medicine, and has good prospects in development and application. The application of the Myriberine A in preparing a medicine for treating breast cancer, disclosed by the invention, is disclosed for the first time, and the inhibition activity of the Myriberine A against breast cancer cells is unexpectedly strong.
CA2428511C Novel uses of combined 5-ht1a agonists and serotonin reuptake inhibitors Use of compounds being combined selective serotonin (5-HT) reuptake inhibitors (SSRIs) and 5-HT1A receptor agonist, in particular 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbomoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof or 3-{4-[4-(4-cyano-phenyl)-piperazin-1-yl]-butyl}-1H-indole-5-carbonitrile or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in veterinary medicine for the treatment or prophylaxis of self directed traumatic disorders associated with behavioral stressors and compulsive disorders associated with behavioral stressors.
EP1320361A4 Method for reducing exacerbations associated with copd This invention relates to a method for reducing the incidences and/or the severity of exacerbations of COPD by administering a phosphodiesterase 4 (PDE4) inhibitor.
EP1233761B1 Osmotic dosage form comprising first and second coats A dosage form is described having a drug core, an inner, fluid-permeable membrane surrounding the drug core, and an outer, semipermeable membrane having exit means formed or formable therein surrounding the inner membrane. The drug core forms a solution with imbibed fluid through the membranes and dissolves the inner membrane over time, thereby furthering the maintenance of controlled, sustained delivery of drug from the dosage form.
CA2754934A1 Substituted 3-aminoisoxazolopyridines as kcnq2/3 modulators The invention relates to substituted 3-aminoisoxazolopyridines, methods for the production thereof, medicaments containing said compounds, and the use of said compounds for producing medicaments.
CN102958508A Ophthalmic devices containing chemokine antagonists Ionic ophthalmic devices, methods of treating chemoattractant cytokine receptor 2 (CCR2) mediated inflammatory conditions, and methods of making such devices are disclosed herein.
WO2010020676A1 The use of topoisomerase type i inhibitors to treat viral infections The present invention relates to the use of compounds, inducing isgylation to treat viral infections. More specifically, the invention relates to topoisomerase type I inhibitors, such as camptothecin and camptothecin derivatives to treat viral infections, preferably infections by RNA viruses. The invention relates further to the measurement of the level of ISG15 and or the level of isgylation during or after treatment as a method to measure the efficacy of the antiviral treatment.
CN102827053A Aromatic amidine derivatives, and preparation method and pharmaceutical application thereof The invention relates to aromatic amidine derivatives, and a preparation method and pharmaceutical application thereof, and discloses a preparation method of a synthesized polypeptide pharmaceutical preparation. The method is characterized by comprising the following steps: dissolving polypeptide in a solvent, evenly mixing with a carrier, spreading a think layer of the mixed solution on a glass dish, putting the glass dish in a drying box, putting a drying agent under the glass dish, and carrying out vacuum drying at 0-40 DEG C until reaching constant weight, wherein the solvent is methanol, ethanol or acetone; the carrier is oligosaccharide, amino acid, empty microcapsule or medicine compounded with polypeptide; and the weight ratio of the polypeptide to the carrier is (0.1-1):1. The preparation method disclosed by the invention is simple, and saves the cost for freeze-drying equipment and operation, thereby greatly lowering the preparation cost and being more beneficial to large-scale industrial production.
US20120315234 Composition for hair and body application The inventive compositions comprise in a deionized water base, a composition comprising: a preservative, a chelating agent; one or more moisturizer and hydrolyzed keratin protein; an antioxidant selected from the group consisting of citric acid and a vitamin E salt; and an emulsifier-water trap selected from the group consisting of cetearyl alcohol and glyceryl stearate; and PEG-40 castor oil. The composition, which is in liquid form, may be applied in the form of a spray or mist by dipping the affected area in the liquid or by pouring a small amount of the liquid onto the hair or body to be treated.
CN101933918A Sarpogrelate hydrochloride sustained-release preparation and preparation method The invention provides a low-release sarpogrelate hydrochloride medicament. The main ingredients of the medicament can be continuously released in the gastrointestinal tract for over 10h.
US20090325974 1,5-diphenylpyrazoles ii as hsp90 inhibitors Novel 1,5-diphenylpyrazole derivatives of the formula (I) in which R1-R6 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
CN101062017B Hyaluronic acid and preparation process thereof The invention discloses a hyaluronic acid particle, which is characterized by the following: comprising a polymer; reacting hyaluronic acid and alkylate with aldolisation; getting the polymer; comprising at least one hydroxide radical in the hyaluronic acid; comprising at least dialdehyde in the alkylate; proceeding aldolisation with the hydroxide radical and aldehyde group; generating crosslinking bridge formation among the hyaluronic acid; crosslinking the hyaluronic acid and alkylate in emulsion; getting the product. This product can be used to hypodermic injection and biological medical treatment.
CN101708161A Elemene injection and preparation method thereof The invention discloses an elemene injection. One liter of the injection consists of the following raw materials: 5 to 20 grams of elemene, 15 to 60 grams of soybean lecithin for injection, 5 to 99.9 grams of oil for injection, 12 to 30 grams of glycerol for injection, and the balance of phosphate buffer solution. The invention also discloses a method for preparing the elemene injection. By controlling the content of lysophosphatide in an auxiliary material, namely soybean lecithin, and key preparation process conditions, an anti-cancer medicament, namely the elemene injection, is prepared, which has no hemoclasis, no vascular irritation and no risk of the survival of microorganisms after the sterilization, is suitable for intravenous injection or arterial intervention, has a dosage form of medicament-loaded emulsions, and is safe and effective.
EP1754475A1 Use of C-terminal modified oxamyl dipeptides as inhibitors of the ice/ced-3 family of cysteine proteases The present invention relates to the use of compounds for formula (I), wherein R1, A, B and R2 are defined herein, for the manufacture of a medicament for the treatment of an infectious disease or an inflammatory condition or for prolonging organ viability for use in transplantation.
EP2414334A1 Bridged bicyclic heterocycle derivatives and methods of use thereof The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
US20110160244 Phenylpiperidine modulators of mu-opioid receptor The present invention relates to new phenylpiperidine modulators of μ-opioid receptors, pharmaceutical compositions thereof, and methods of use thereof.
US20120157403 Bicyclic and tricyclic derivatives as thrombin receptor antagonists Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
US20050159476 Pharmaceutical composition for preventing or treating respiratory disease An object of the present invention is to provide a pharmaceutical composition and a method for preventing or treating a respiratory disease. The pharmaceutical composition comprises a compound represented by formula (1): or a pharmaceutically acceptable salt thereof as an active ingredient.
CN1879753A Medicine for treating diabetes of blood stasis complicated kidney spleen deficiency type Disclosed is a medicament for treating diabetes, which is prepared from red ginseng, chicken's gizzard-skin, prepared rehmannia root, cornus officinalis, astragalus root, atractylodes rhizome, root of red rooted saliva and Cinnamomum cassia, as well as western medicament including Gliclazide, Metformin, and microelements including Cr, Se, Znand V.
CN101848715A Two-component eye drops containing pirenoxine Two-component eye drops to be mixed before using which comprise a pirenoxine-containing suspension and a dissolution liquid. Compared with eye drops of the existing type wherein pirenoxine tablets or granules are dissolved by using a dissolution liquid before using, the above-described eyedrops are characterized in that the dissolution time of pirenoxine can be shortened. The eyedrops are also characterized in that transparent eyedrops having a physiologically acceptable pH value at a weakly acidic to neutral level can be obtained after dissolving pirenoxine.
EP1761519B1 Indole derivatives as histamine receptor antagonists The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
US20090226551 Pharmaceutical composition for prevention and/or treatment of bone loss A pharmaceutical composition for preventing and/or treating bone loss is disclosed. The pharmaceutical composition includes an effective amount of a licorice, black bean, Cnidi Fructus, and buckhorn.
WO2014069626A1 Method for producing pyrimidodiazepinone compound Provided is a method for producing a compound represented by formula (I) (wherein R1 and R2 may be the same or different and each represents a hydrogen atom or the like, and Z represents an optionally substituted aryl group or the like) or a salt thereof, or the like. The production method comprises: (i) a step wherein a compound represented by formula (II) (wherein R1 and R2 are as defined above, R3 represents a lower alkyl group, and X represents a halogen atom or the like) is reacted with a compound represented by formula (III) (wherein Z is as defined above) or a salt thereof in the presence of a base, thereby obtaining a compound represented by formula (IV) (wherein R1, R2, R3 and Z are as defined above) or a salt thereof; and (ii) a step wherein the compound represented by formula (IV) or a salt thereof is processed with an acid or a base, thereby obtaining a compound represented by formula (I).
WO2009022171A1 Pyridinyiioxy pyridines as alk5 inhibitors The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess ALK5 (TGFβRl) inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti¬ cancer effect in a warm-blooded animal such as man.
CN101385712A Mouth spray for preventing and treating nausea and emesis after tumor chemotherapy and radiotheraphy and preparation method thereof The invention relates to an oral spray for controlling nausea and vomit of chemotherapy and radiation therapy, the formula of the oral spray is composed of ingredients with the following parts by weight: 5-50 parts of drug absorption enhancer, 2-20 parts of drug active ingredient and 30-90 parts of buffer, the drug absorption enhancer can be any one or the combination of more of the following ingredients: azone, propylene glycol, polysorbate (Tween), ethylene glycol deoxycholic acid sodium salt, brij, sodium decanoate, lauric acid, stearic acid, sodium lauryl sulphate, stearyl alcohol sodium sulfate, dioctyl succinate sodium sulfonate, oleic acid, GK2, menthol and borneol; the drug active ingredient can be any one combination of the following ingredients: palonosetron hydrochloride, granisetron, ondansetron, azasetron and tropisetron; and the ingredients of the buffer are sodium citrate buffer solution and phosphate buffer solution. The oral spray provides a formulation which is safer, painless and convenient for patients with advanced tumor, elderly and weak patients, children patients and the patients who suffer from the metal illness and do not obey the oral administration or the injection drug administration.
EP1200040B8 Two-component composition for cosmetic or pharmaceutical use The present invention relates to a biphasic composition for cosmetic or pharmaceutical use comprising antioxidants and beneficial compounds for the skin, such as moisturizers and immunomodulators. The composition comprises ascorbic acid as the antioxidant compound and ceramides as the selected moisturizing agent and betaglycane as the immunomodulator, presenting a low potential risk for sensitization and having effective antioxidant action, in addition to an outstanding sensitive effect.
CN103183684A Quinolone lactone compound, and preparation method and application thereof The invention discloses a quinolone lactone compound and a preparation method and an application thereof. The quinolone lactone compound has a structural formula shown a formula (II) and is prepared through an intramolecular cyclization reaction by putting a quinolone derivative shown as a formula (I) in a microwave reactor under an alkali condition. The quinolone lactone compound has a good antibacterial effect and can be used for preparing bacteriostatic agents.
US20110201618 Kmups inhibiting proliferation and obliteration of pulmonary artery An obstructive pulmonary disease inhibiting pharmaceutical composition is provided. The obstructive pulmonary disease inhibiting pharmaceutical composition includes: an effective amount of a compound of formula I, wherein R2 and R4 are each selected independently from the group consisting of a C1˜C5 alkoxy group, a hydrogen, a nitro group, and a halogen atom; and a pharmaceutically acceptable carrier.
CN1850045A Slow-release preparation containing macrolides anti biotics The present invention relates to a slow-released preparation containing macrolide antibiotics. Said slow-released preparation is slow-released injection or slow-released implant preparation. Said injection is composed of slow-released microsphere and solvent, said slow-released microsphere contains slow-released auxiliary material and macrolide antibiotics, the solvent is special solvent containing suspension adjuvant of carboxymethyl cellulose sodium, its viscosity is 100 cp-3000 cp (20 deg.C-30 deg.C); the slow-released auxiliary material is selected from EVAc, PLA, PLGA, sebacic acid copolymer, albumin glue and golatin, etc. The slow-released implant preparation is prepared by using slow-released microsphere or adopting melting process. Said invention also provides its application method, and can obtain obvious therapeutic effect for curing various infective diseases.
US20110059955 Novel 3-aminoalkyl-1,3-dihydro-2h-indol-2-one derivatives, preparation thereof and therapeutic use thereof The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application. The compounds of the present invention correspond to the formula (I): in which the variables are as set forth in the specification. These compounds exhibit a strong affinity and a high selectivity for human arginine-vasopressin (AVP) V1a receptors and some compounds additionally exhibit a strong affinity for AVP V1b receptors.
CN202288921U Compound naproxen esomeprazole tablet The utility model discloses a compound naproxen esomeprazole tablet, which comprises a film-coating layer I and a naproxen esomeprazole bilayer tablet II, the film-coating layer I directly wraps the bilayer tablet II, wherein the naproxen esomeprazole bilayer tablet II is formed by an upper layer and a lower layer which consist of a naproxen tablet layer III and an esomeprazole tablet layer IV. The two medicines of the compound naproxen esomeprazole tablet are ensured to be dissolved out at the same time, the dose is easy to control, the tablet appearance is smooth and attractive, the tablet is easy to swallow, and the medicine taking complicance of a patient is improved.
CN103054888A Solid oral preparation containing acarbose and atorvastatin calcium and preparation method of solid oral preparation The invention discloses a solid oral preparation containing acarbose and atorvastatin calcium. The solid oral preparation comprises acarbose and atorvastatin calcium, wherein the weight ratio of the acarbose to the atorvastatin calcium is (5-80): (20-200); and the solid oral preparation further comprises pharmaceutically acceptable excipients, wherein the weight ratio of the atorvastatin calcium to the excipients is 1: (2.3-30). The invention further discloses a preparation method of the solid oral preparation. The invention has the beneficial effects that the blood glucose and the blood lipids can be reduced synergistically, the cholesterol and triglyceride can be lowered while the blood glucose is reduced, the high-density lipoprotein (HDL) level in the blood can be increased, and the hypoglycemic and hypolipidemic effects can be improved, thereby correcting the metabolic syndrome of diabetics and reducing the long-term risk of cardiovascular and cerebrovascular diseases of the diabetics.
US20110098273 Oligomer-Calcium Channel Blocker Conjugates The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
US20080220003 C5a Receptor Antagonists The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (—CONH2), substituted carbamoyl, carboxyl, carbamate, alkoxycarbonyl, substituted alkoxycarbonyl, acylamino, substituted acylamino, sulfamoyl (—SO2NH2), substituted sulfamoyl, haloalkyl, haloalkyloxy, —C(O)H, trialkylsilyl and azido.
CA2651979A1 Triazolopyridazine derivatives The invention relates to compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and R3 ' are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula (I).
US20130045194 Delivery of Cholesteryl Ester to Steroidogenic Tissues Disclosed are compositions and methods for treating conditions characterized by low HDL-CE which can lead to decreased delivery of cholesteryl ester to steroidogenic tissues, reducing the organ's ability to produce steroids especially during periods of demand, stress and or systemic inflammatory response syndrome.
WO2008018371A1 Oral disintegrating tablet having masked bitter taste and method for production thereof Provided is an oral disintegrating tablet comprising mitiglinide calcium hydrate, which shows reduced bitter taste and rapid disintegrating properties in an oral cavity and can be dissolved in a digestive tract rapidly. The oral disintegrating tablet comprises a) mitiglinide calcium hydrate, b) crystalline cellulose, c) at least one member selected from the group consisting of an aminoalkyl methacrylate copolymer E, polyvinylacetal diethylaminoacetate, an ethyl acrylate/methyl methacrylate copolymer and ethylcellulose as a masking agent, d) a sugar or a sugar alcohol, and e) at least one member selected from corn starch and partially gelatinized starch, and has masked bitter taste.
DE102005023640A1 Active substance combination, useful for skin moisturizing and stabilization of skin barrier, comprises glucosylglycerides and partially neutralized esters of monoglyceride and/or diglyceride fatty acids with citronic acids Active substance combinations comprises one or more of glucosylglycerides and one or more of partially neutralized esters of monoglyceride and/or diglyceride fatty acids with citronic acids. An independent claim is included for a cosmetic preparation comprising the active substance combination.
CN103070825A Curcumin particle suspension used for intramuscular injection and hypodermic injection, preparation method and application The invention discloses a curcumin particle suspension having a slow release effect used for intramuscular injection and hypodermic injection, and a method for preparing the suspension used for injection. An auxiliary material of the curcumin particle suspension used for injection contains no solubilizer or cosolvent, the security is good; the curcumin particle suspension can reach slow release effect through hypodermic and intramuscular injection administration, the stability of the curcumin particle suspension is good, and the curcumin particle suspension can be used in industry.
WO2013106702A1 Halofuginol derivatives and their use in cosmetic and pharmaceutical compositions The present invention provides halofuginol, and derivatives and salts thereof, including diasteromerically enriched compositions thereof. The invention also provides pharmaceutical and cosmetic compositions thereof as well as methods for using halofuginol and derivatives thereof in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, malaria, ischemic damage, transplant rejection, neurodegenerative diseases, T-cell neoplasms, and cosmetic conditions.
WO2007005177A1 Alpha-2 adrenergic agonists for the treatment of pain A compound is disclosed herein comprising Formula or a pharmaceutically acceptable salt, metabolite, or prodrug thereof; wherein R1, R2, and R3 are independently hydrogen or C1-4 alkyl; A is OH, NH2, or SH; and n is 0, 1, or 2. Methods, compositions, and medicaments related thereto are also disclosed.
WO2007016012A3 CYCLOALKYL AMINO-HYDANTOIN COMPOUNDS AND USE THEREOF FOR β-SECRETASE MODULATION The present invention provides a 2-amino-5-cycloalkyl-hydantoin compound of formula (I) The present invention also provides methods and compositions for the inhibition of ß-secretase (BACE) and the treatment of ß-amyloid deposits and neurofibrillary tangles.
CN103284969A Risperidone dispersible tablet and preparation method thereof The invention discloses a risperidone dispersible tablet and a preparation method thereof. The preparation is formed by evenly mixing and tabletting medicine-carrying particles and pharmaceutically acceptable auxiliary ingredients, the medicine-carrying particles are prepared by adopting the following method: dissolving risperidone into absolute ethyl alcohol, adding Kollidon CL-M, drying, removing ethanol, and sieveing. The risperidone dispersible tablet is short in disintegration time, the settling volume ratio meets the specification, and the risperidone dispersible tablet can be dissolved out completely.
CN101574319A Podophyllotoxin vesicle and preparation method thereof The invention relates to a podophyllotoxin vesicle and a preparation method thereof. The preparation method takes a non-ionic surfactant and modification lipids as vesicle materials, and adds cholesterol, dicetyl phosphate and the like as stabilizers. The vesicle having the advantage of good preparation stability is a novel preparation easy to industrialize.
CN102838523A Anti-enterovirus 71 (EV71) valerolactam compounds, preparation method and uses thereof The invention relates to valerolactam enterovirus 71 (EV71) 3C protease inhibitors, wherein a structure general formula of the inhibitors is represented by a compound M, various variables in the structure is defined in an instruction, and EV71 replication is effectively inhibited or blocked with the compounds. The present invention relates to discoveries and applications of the compounds containing the structure represented by the formula (M), optical isomers, metabolites with pharmaceutical activities, pharmaceutically acceptable salts, solvates, and prodrugs thereof in preparations of anti-virus drugs for treatment of hand-foot-mouth disease infection. The present invention further relates to an intermediate of the structure compound represented by the formula (M) and a synthesis method thereof.
CN101919999A Tea-ginger-vinegar medicament The invention relates to a tea-ginger-vinegar medicament belonging to the field of weight loss and health care. The tea-ginger-vinegar medicament overcomes the defect that no tea-ginger-vinegar medicament exists in the market. The tea-ginger-vinegar medicament is mainly characterized by being prepared by concentrating tea, ginger and vinegar. The tea-ginger-vinegar medicament can be used for weight loss and health care.
US7504507 carboxamide linked compounds based on benzo[b][1,6]naphthyridin-1 (2H)-one, which differ from previous acridine based compounds by the incorporation of a lactam or thiolactam function in one of the outer rings This invention relates to polycyclic carboxamide compounds of the formula (I) with cytotoxicity, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly I the treatment and/or prophylaxis of cellular proliferative disorders such a cancer.
WO2012078757A3 Combination for breast cancer therapy with hsp90 inhibitory compounds Methods for treating breast cancer, comprising administering to the subject an effective amount of a selective estrogen receptor modulator and an effective amount of a compound represented by the following structural formula: (I) (Ia) a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein.
US20110097423 Gene Prognosis Predictor Signature for Colorectal Carcinoma The present invention is drawn to methods of assessing colorectal cancer prognosis by examining the expression of particular genes disregulated in this disease state. Subjects exhibiting disregulation in one or more of these genes will have a higher risk of cancer recurrence and death.
US20100203117 Anti-adipogenic compositions containing piper betle and dolichos biflorus Herbal compositions are useful for inhibition, amelioration or prevention of adipogenesis mediated diseases such as obesity, lipid storage disease and hyperlipemia. The herbal compositions comprise biologically effective amounts of extracts or fractions from Piper betle in combination with one or more of the extracts or fractions derived from Dolichos biflorus, Commiphora mukul, Boerhaavia diffusa, Tribulus terrestris and Zingiber officinale as active ingredients. The compositions optionally contain a bio-enhancing agent or a bio-protecting agent, along with biologically acceptable carriers or diluents. The herbal compositions may be used in a method for treating or preventing adipogenesis involved diseases in mammals.
EP1079843B1 Use of alfa1beta1 integrin receptor inhibitors and tgf- beta1 inhibitors in the treatment of kidney disease The present invention provides methods for treating (i.e., delaying the onset of, slowing the progression of, and/or reversing) kidney disorders (e.g., renal glomerulonephritis and/or renal fibrosis). Certain of these methods involve administering an α1β1 integrin receptor inhibitor optionally in combination with a TGF-β1 inhibitor. The present invention also provides a mouse model for kidney disease wherein the mouse does not express a normal collagen type 4 composition in the GBM (i.e., it does not incorporate collagen α3(IV), α(IV), and α5(IV) chains into its glomerular basement membrane) and does not express the α1β1 integrin receptor.
CN102558153A Novel pharmaceutical salt of dabigatran etexilate and preparation method thereof The invention relates to a novel pharmaceutical salt of dabigatran etexilate. The novel pharmaceutical salt comprises benzenesulphonate, maleate, benzoate, oxalate, lactate, fumarate, tartrate, and the like. Combined with auxiliary materials, the novel pharmaceutical salt can be prepared into oral preparations including granules, common tablets, dispersible tablets, oral disintegrating tablets, sustained-release tablets, capsules, sustained-release capsules, and the like. The operations can be used in clinical anticoagulation treatments.
US20120108596 Aza-Bicyclic Amine N-Oxide Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligand Pro-Drugs The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
CN1965817A Sustained release tablet of glibenclamide and preparation process thereof The invention relates to a Glibenclamide slow release tablet preparation which comprises effective dose of main constituent of Glibenclamide and medicinal auxiliary materials, the constituents include (by weight portion) Glibenclamide 0.5-5.0 parts, slow release material 20.0-170.0 parts, filling agent 5-100 parts, lubricating agent 5.0-30.0 parts, and right amount of binding agent. The invention also discloses the process for preparing the tablet preparation.
US20060051439 comprises acerola seed extract containing quercitrin The invention relates to antioxidants that make effective use of acerola seeds, which have conventionally been discarded, that have high safety and excellent antioxidative effect in skin preparations for external use, cosmetics, and food, and that contain acerola seed extract as an active component. The invention also relates to skin preparations for external use, cosmetics, and food containing the antioxidant.
EP1685876A1 Solid cosmetic cleansing composition Skin cleaning composition (A), in solid form, comprises an active compound (I) of salicylic acid or its derivatives, an anionic surface-active foaming powder (II) and a water-soluble polymer (III) (10 wt.%), in an anhydrous medium. Independent claims are included for: (1) a sponge comprising (A); and (2) a cosmetic cleaning process comprising wetting (A) or the sponge with water, to pass on the skin and rinsing the skin. - ACTIVITY : Antiseborrheic; Dermatological. - MECHANISM OF ACTION : None given.
CN102846648A Veterinary drug for treating infectious coryza of chicken The invention discloses a veterinary drug for treating infectious coryza of chicken, and is characterized in that the veterinary drug comprises tylosin tartrate, ciprofloxacin hydrochloride and glucose. The inventive veterinary drug can effectively treat infectious coryza of chicken, has evident curative effect and convenient application, and deserves wide generalization.
US20070167402 Product of coprecipitation of sparingly soluble substance and water-soluble polymer and process for producing the same The present invention provides a coprecipitate of 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H), 10-dio xo-2H-1,2,3-triazolo[4,5-c][1]benzazepine and a water-soluble polymer, excellent in solubility and absorbability.
CN201410116Y Amoxicillin and sulbactam pivoxil dual-release capsule The utility model relates to an amoxicillin and sulbactam pivoxil dual-release capsule which comprises a capsule casing and a pharmaceutical preparation filled in the capsule casing, wherein the pharmaceutical preparation adopts sulbactam pivoxil fast release tablets and amoxicillin sustained-release tablets. The preparation solves the problem that beta-lactamase generates drug resistance after amoxicillin is taken, enables the amoxicillin to be prepared into gastric floating sustained-release tablets, prolongs the time of drug action, increases the drug absorption, and enhances the bioavailability.
US20100168166 Method of Providing An Antihistaminic Effect in a Hepatically Impaired Patient The present invention relates to a method of providing an antihistaminic effect in a hepatically impaired patient in need thereof comprising administering to said patient an effective antihistaminic amount of a compound of the formula wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A and B is hydrogen or hydroxy with the proviso that at least one of A or B is hydrogen; or a pharmaceutically acceptable salt and individual isomers thereof.
US20080213385 Formulations for 7- (T-Butoxy) Iminomethyl Camptothecin The present invention relates to nanoparticulate compositions in which the active agent is a topoisomerase I inhibitor and pharmaceutical compositions comprising the nanoparticulate compositions that are useful for the treatment and prevention of proliferative diseases including cancer.
CN103435606A CDK2 and CSK3beta dual inhibitor and application thereof The invention relates to the field of medicinal chemistry, and particularly relates to compounds (1-24) and medical applications of medicinal compositions containing the compounds, especially applications of the medicinal compositions serving CDK2 and CSK3beta dual inhibitors.
CN101057996A Rapamycins coating catheter The invention discloses a catheter coated with rapamycin. The outer surface of part catheter is coated with catheter. It is used for preventing disease recurrence for urine injured patient or urethral stricture patient.
WO2006082707A1 Immune enhancer A high-molecular weight polysaccharide containing an arabinogalactan moiety comprising D-galactose, an arabinoxylan moiety comprising D-xylose, an arabinan moiety comprising L-rabinose and a glucan moiety comprising D-glucose. An immune enhancer comprising this high-molecular weight polysaccharide more clearly participates in immunopotentiation by, for example, activating macrophages.
WO2002057256A9 Piperazinylcarbonylquinolines and -isoquinolines Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT¿2A? antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Hutington's disease, eating disorders, such as bulimia, anorexia nervosa, premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).
CN101891730A Synthesizing method of 7-alkoxy methyl hesperetin and pharmaceutical use thereof The invention relates to a novel chemical which has the chemical name of 7-alkoxy methyl hesperetin derivative and has the following molecular structural formula, wherein R is CnH2n+1, and the n is from 1 to 20. The novel chemical has anti-inflammatory activity obviously higher than that of the hesperetin and has higher medicinal value.
CN101933968A Pharmaceutical composition with functions of resisting oxidation and delaying senility and preparation method thereof The invention relates to a pharmaceutical composition with functions of resisting oxidation and delaying senility and a preparation method thereof. The pharmaceutical composition is prepared by mixing supplementary materials of soybean isoflavone, pueraria extracts, vitamin C, and the like according to a certain proportion. The pharmaceutical composition has the effects of resisting oxidation and delaying senility.
US20120122944 Tetrahydronaphthalene derivatives This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.
US20090258909 Novel Benzimidazole Derivatives Useful as Selective Androgen Receptor Modulators (SARMS) The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
CN101953774A 2-methoxy estradiol injectable hydrogel implant The invention relates to a 2-methoxy estradiol injectable hydrogel implant which can effectively solve the problems of maintaining the effective concentration of the target part of 2-methoxy estradiol and enhancing the treatment effect. The invention has the technical scheme that a temperature sensitive type PLGA-PEG-PLGA segmented copolymer having temperature sensitive hydrogel properties is adopted to be mixed with water to prepare dissolution swelling solution; the solution is mixed with the 2-methoxy estradiol to prepare an injection; the temperature sensitive type PLGA-PEG-PLGA segmented copolymer is uniformly mixed with the water to be kept stewing at 0 to 25 DEG C; the temperature sensitive type PLGA-PEG-PLGA segmented copolymer is fully dissolved and swelled into the solution; and the 2-methoxy estradiol is added to be uniformly mixed with solution at 0 to 25 DEG C on the use day or one day before use. The invention has scientific formula, easy production, low cost and good injection effect, can effectively maintain the effective concentration of the target part of the 2-methoxy estradiol and enhance the treatment effect is enhanced and is the innovation on the path of cancer treatment drug forms and drug administration.
CN101695478B Tamsulosin hydrochloride sustained-release pellets and preparation method thereof The invention discloses tamsulosin hydrochloride sustained-release pellets, which are prepared by coating medicament-containing blank pellets, wherein the blank pellets contain microcrystalline cellulose, soluble starch, lactose and croscarmellose sodium. Two layers of coating liquid are a Surelease sustained-release coating material and an enteric-coating material Kolicoat MAE 30DP respectively and the tamsulosin hydrochloride sustained-release pellets are capsules. The tamsulosin hydrochloride sustained-release pellets of the invention adopt the sustained-release coating material and the enteric-coating material to control the release of medicaments. The prepared tamsulosin hydrochloride sustained-release pellet capsules release less than 40 percent of medicaments in hydrochloric acid solution with a pH value of 1.2 in two hours and release 40 to 70 percent (about 60 percent) of medicaments in phosphate buffer solution with a pH value of 6.8 in three hours and over 70 percent (about90 percent) of medicaments in five hours, so the prepared tamsulosin hydrochloride sustained-release pellet capsules meet the requirements of quality standards. The invention discloses a preparation method of the tamsulosin hydrochloride sustained-release pellets.
WO2009053548A1 Rimonabant 1,4-dioxane solvate, method for preparing same and pharmaceutical compositions containing same The invention relates to a rimonabant 1,4-dioxane solvate, to a method for preparing the same and to the therapeutic uses thereof.
EP1283725B1 Solid dispersion system of pranlukast with improved dissolution, and the preparing method thereof The present invention relates to a novel composition of pranlukast, of which solubility in aqueous media is low, method for producing said composition and oral preparation comprising said composition. More specifically, the present invention is related to oral solid dispersion composition of pranlukast with improved dissolution characterized in comprising (A) pranlukast and (B) at least one polymer selected from a group consisting of hydroxypropylcellulose and hydroxypropylmethylcellulose; method for preparation thereof; and oral preparation prepared thereby.According to the present invention, pranlukast solid dispersion composition with high oral absorption rate via improvement in dissolution thereof can be obtained. The pranlukast solid dispersion composition of the present invention exhibits high dissolution rate under in vitro dissolution condition, and improved absorption rate upon oral administration to human.
CN101999553A Feed additive for controlling livestock sand crack The invention relates to a feed additive for controlling livestock sand crack, which comprises the following raw materials in percent by weight: 18-21 percent of fat powder, 6-8 percent of zinc fumarate, 1-3 percent of biotin, 0.3-0.5 percent of vitamin B2, 0.2-0.3 percent of pantothenic acid, 0.2-0.3 percent of folic acid, 0.08-0.2 percent of ethoxy quinoline and 68-72 percent of carrier. 0.2 percent of additive is added in the daily base feed of pigs, thus the incidence rate of noncommunicable and nontransmissible livestock limb and foot diseases can be remarkably reduced, and the sand crack disease of the livestock can be effectively treated.
CA2763041A1 Compositions and methods for modulating lipid composition The present subject matter relates to a novel herbal and oil composition and methods for modulating fatty acid composition and metabolism in an animal. In one aspect, the subject matter involves a composition comprising rosemary extract, oregano extract, and a polyunsaturated oil. In a particular embodiment, the polyunsaturated oil is fish oil or a derivative thereof. In some embodiments, the present subject matter relates to methods for modulating essential dietary fatty acid composition of lipoprotein particles or cell membranes, modulating essential fatty acid metabolism, regulating the activity of lipoxygenases and cyclooxygenases, improving cardiovascular health, and / or inhibiting cell proliferation diseases and disorders.
US20080183250 Compositions and methods for treating or preventing skin inflammation via restoration of skin barrier function Compositions, kits and methods are provided for restoring skin barrier function to skin of a subject after a medical or a cosmetic procedure. In general, a composition containing divalent cations such as calcium ions and/or magnesium ions in a physiologically acceptable medium can be used to treat, inhibit or prevent inflammation of skin post medical, demertological, or cosmetic procedure such as chemical peeling, laser skin resurfacing, microdermabrasion, plasma energy treatment, radiofrequency treatment, hair or vein removal or lightening, skin treatment using light energy or photofacial, thereby treating, inhibiting or preventing post-inflammatory hyperpigmentation of the skin or other skin disorders.
US20090318439 5-furopyridinone substituted indazoles Compounds are disclosed. The compounds act as MCH1 modulators. Other embodiments are also disclosed.
WO2011126733A3 Combination therapies: inhibitors of gaba transaminase and nkcc1 Inhibitors of NKCCl, such as bumetanide, when coadministered with inhibitors of GABA transaminase, such as vigabatrin, attenuate both the retinal toxicity and the intramyelinic edema.
WO2013122554A1 Pellet formulations comprising esomeprazole The present invention relates to stable pharmaceutical formulations comprising esomeprazole and production method of these formulations in order to be used in diseases induced by gastric acid secretion disorder.
EP2090309A1 Use of thiazole inhibitors of fatty acid oxidation of formula (I) for the treatment of Alzheimer's disease and other neurological conditions Methods for inhibiting and/or reversing tau filament formation or polymerization are provided. These methods can be used for treating certain neurological disorders in vivo by administering pharmaceutical compositions which inhibit and/or reverse tau filament formation or polymerization. An especially preferred pharmaceutical composition contains an inhibitor of the general formula (I), wherein R1 is an aliphatic radical having one to six carbon atoms and wherein R2 and R3 independently are a second aliphatic radical having one to six carbon atoms, a hydroxyl-substituted aliphatic radical having one to six carbon atoms, or a pheny radical or a pharmaceutically acceptable salt of the inhibitor.
CN102836136A Indiplon orally disintegrating tablet and preparation method thereof The invention belongs to the medical field of medicine, and particularly discloses an indiplon orally disintegrating tablet, which has a good taste, dispenses with water when being taken, can be rapidly disintegrated after entering the mouth, is suitable for being taken by dysphagia patients such as the old people and children and is also suitable for being taken under the condition that water sources are difficult to obtain, such as during a journey or wartime. The indiplon orally disintegrating tablet is sedative-hypnotic taken before bedtime, dispenses with the water when being taken, can prevent the phenomenon that the sleep quality is influenced by micturition desire after the medicine is taken by using water before the bedtime, and has good medicine taking compliance. The invention also discloses a preparation method of the indiplon orally disintegrating tablet, which has the advantages that a process is simple, the cost is low, the prepared orally disintegrating tablet is disintegrated fast and acts rapidly, and the medicine taking discomfort of a patient is reduced.
WO2012106287A8 Methods of treating acute kidney injury with retinoic acid The present invention provides, in one embodiment, a method of inhibiting apoptosis in kidney epithelial cells after acute injury by modulating/inhibiting Nur77 induction/expression or function/activity in the cells. The invention further provides a method of preventing or treating an acute kidney injury in a subject in need thereof, comprising administering to the subject an effective amount of a retinoic acid or retinoic acid derivative, and a method of preserving a kidney for transplant, comprising contacting the kidney with a solution that comprises a retinoic acid or a retinoic acid derivative.
CN101108188A Novel long circulation alprostadil liposome drug feeding system for injection and method of preparing the same The invention provides an alprostadil macrocyclic lipidosome drug delivery system for intravenous injection, which comprises effective dosage of prostaglandin E1, polyethyleneglycol derivative phospholipid, cholesterin and pharmaceutically acceptable supplementary materials. The invention is prepared with the method that: wrap the drug in a formed lipid double-layer film to prepare a prostaglandin E1 lipidosome drug delivery system. After the formation of the lipidosome, the long chain of polyethyleneglycol can be dispersed on the surface of particle to form a hydrophilic protection film, which can prevent the cluster of particle, prevent the recognition and phagocytosation by reticular system in the body, prolong the preservation duration of the particle drug delivery system in blood circulation and realize the macrocycle. Besides, because the drug is wrapped in the lipidosome, the drug can be protected from the damage caused by external factors (i.e. water, oxygen and light), so as to greatly enhance the stability of drug during the storage process.
US20120184600 Inhibition of Glycerol-3-Phosphate Acyltransferase (GPAT) and Associated Enzymes for Treatment of Viral Infections A method of treating or preventing a viral infection in a mammal by administering a compound or pharmaceutically acceptable derivative thereof that inhibits a phosphatidic acid synthesis enzyme
EP1401439B1 Use of bicyclo compounds for treating alzheimer's disease Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula (I) wherein X, Y, Z, R?1, R2, and R3¿ are defined herein.
US7122538 Neuroleptic agents for treating schizophrenia, psychological disorders, depression; 5-(4-Chlorophenyl)-thiophene-2-sulfonic acid (8-methoxy-3-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)amide The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR5R6, —SO2NR5R6, —(CH2)NR5R6, —(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring; R3 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8 or —(CH2)pNR7COR8; R4represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, trifluoromethyl, trifluoromethoxy, halogen, —OSO2CF3, —(CH2)pC3-6cycloalkyl, —(CH2)qOC1-6alkyl or —(CH2)pOC3-6cycloalkyl; R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; R7 and R8 each independently represent hydrogen or C1-6alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; q independently represents an integer selected from 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that the compounds 8-hydroxy-3-methyl-7-phenylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 8-hydroxy-7-4-(hydroxyphenyl)sulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline and 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline hydrochloride are excluded. The compounds are useful in therapy, in particular as antipsychotic agents.
WO2014127418A1 Conjugate compound and uses of same Conjugate compounds of hyaluronic acid bonded to pentosan poiysulfate, or salts or derivatives thereof, are shown to induce chondrogenic differentiation of a population of mesenchymal stem celis as observed by, amongst other indications, increased glycosaminogSycan (GAG) production.
US20110112182 Design, synthesis and functional characterization of rottlerin analogs A method of synthesizing rottlerin analogs is described. The synthesis methods described are the first known method of synthesizing rottlerin analogs from commercially-available materials to produce cost effective analogs. Rottlerin analog structures made by the synthesis methods and methods of use for treating a neurological or inflammatory response mediated by protein kinase C (PKC) are further described.
WO2014122074A1 Combination of nitroprusside and a sulfide salt as an hno-releasing therapeutic for the treatment or prevention of cardiovascular diseases The present invention relates to the combination of a nitroprusside salt or a solvate thereof with a sulfide salt or a solvate thereof for use in the treatment or prevention of a cardiovascular disease/disorder, such as heart failure, heart attack or hypertension.
US20080269280 Antiinflammatory agents; rheumatic diseases; multiple sclerosis Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
US20110105518 Therapeutic agent for spinal canal stenosis The main object of the present invention is to provide a novel agent for the treatment of spinal canal stenosis. The present invention relates to an agent for the treatment of spinal canal stenosis containing the heterocyclic derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient; In the formula (1), R1 and R2 are the same or different and each represents an optionally substituted aryl; R3 and R4 are the same or different and each represents hydrogen atom or alkyl; R5 represents hydrogen atom, alkyl or halogen atom; Y represents N or N→O; A represents NR6, and R6 represents hydrogen atom, alkyl, etc.; D represents alkylene or alkenylene which is optionally substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, etc.; and Q represents carboxy, alkoxycarbonyl, etc.
WO2014164395A1 Combination anti-estrogen receptor cancer therapy using muc1 peptides and chemotherapeutics The invention provides for treatment of MUC1+/ERα+/- cancers using an anti-MUC1 therapy, optionally including an anti-ERα therapy. In particular, the invention addresses the treatment of tamoxifen-resistant cancers, using MUC1+, and optionally anti-ERα therapy.
US7147864 Administering a wound healing agent containing selegiline and/or desmethylselegiline to a subject suffering from photodamaged skin, injury or wound, for a duration sufficient to promote epithelization of such wound The present invention is directed to methods that can be used in the treatment of wounds, burns, and photodamaged skin. Methods can be used for both humans and animals and involve the administration of compositions containing selegiline and/or desmethylselegiline.
US20110319380 Compounds for Treating Disorders Mediated by Metabotropic Glutamate Receptor 5, and Methods of Use Thereof Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
EP2000462A2 Non-imidazole alkylamines as histamine H3-receptor ligands and their therapeutic applications The present invention provides new non-imidazole alkylamine derivatives, and their use for preparing medicaments acting as ligands at the H3-receptors of histamine.
US7547439 Elicit immune response from human lymphocytes when complexed with a major histocompatibility complex molecule type HLA-A2; polypeptide Polypeptides comprising an unbroken sequence of amino acids from SEQ ID NO: 1 or 2, with an ability to complex with a major histocompatibility complex molecule type HLA-A2, and preferably HLA-A2.1.
EP1652849A1 Novel hydrophilic analogs of 4,8-dihydrobenzodithiophene-4,8-diones as anticancer agents The present invention discloses hydrophilic derivatives of 4,8-dihydrobenzodithiophene-4,8-diones of formula (D) or (E) which are active as anticancer agents, along with pharmaceutical formulations containing the same.
CN101070322A 7-(4-nitroyl-3-amino-1-piperidyl) quinolinecarboxylic acid derivative, its preparing method and use This invention relates to 7 - ( 4 - isonitroso - 3 - amido - 1 - piperidyl) new quinoline carboxylic acid ramification and preparation method, and relates to the medicine use, such as antimicrobial and feed additive. More concretely, the invention relates to new fluorine Quinolone and naphthyridine ketone methanoic acid ramification as formulae (I), which has ( 4 - isonitroso - 3-amido - 1 - piperidyl) substituent group at caryo 7 position of quinolone. Comparing with existing fluorine quinolone antibacterial, the invention has superior grampositivebacteria resisting activity and broad spectrum antibacterial activity. Each group definition of the formulae is described in specification.
US20100267700 Immunosuppressive agent and anti-tumor agent comprising heterocyclic compound as active ingredient A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is disclosed. A novel heterocyclic compound represented by the general formula (II) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is also disclosed.
CN101053562A Otilonium bromide capsule The present invention discloses a medical composition comprising effective amount of otilonium Br for treating irritable bowel syndrome or stomach convulsion. Said composition will disperse into small granules within five minutes in water and the in vitro dissolve-out will be above 90%, which will hence dispel the convulsion rapidly. The preferred composition is of capsule type.
US20110224133 Highly Potent Peptides To Control Cancer And Neurodegenerative Diseases This invention provides compositions and method of diminishing or inhibiting autophagy by administering a FLIP protein that binds to Atg3, interfering with the formation of the LC3-Atg4-Atg7-Atg3 conjugation complex necessary for autophagy induction. This invention also provides FLIP peptide fragments that promote or induce autophagy by interfering with the activity of FLIP.
US7071344 Vitamin D derivatives with cyclopropyl rings in the lateral chains, a method and intermediate products for the production thereof and the utilization thereof for producing medicaments The invention relates to novel vitamin D derivatives of general formula (I), a method for the production thereof, intermediate products of the method and the utilization of vitamin D derivatives for producing medicaments.
CN102218042A Sustained release tablet of quetiapine fumarate composition and preparation method of sustained release tablet The invention discloses a sustained release tablet of a quetiapine fumarate composition, comprising the following components in percentage by weight: 25 to 40% of quetiapine fumarate, 2 to 8% of organic acid salt, 5 to 30% of a sustained release material and the balance of other pharmaceutical adjuvants, wherein the sustained release material is K type hydroxypropyl methylcellulose. The sustained release material is the K type hydroxypropyl methylcellulose and the organic acid salt is added, therefore, a stable sustained release skeleton can be formed by few sustained release materials, the raw material can be saved, the weight of unit preparation can be reduced, and the problem of difficulty in swallowing caused by large size of the preparation can be released and/or solved; the hydroxypropyl methylcellulose with different viscosities are used as the material of the skeleton so that the preparation can reach formulated sustained release effects and has the characteristics of strong controllability and stability in storage. By use of the preparation method capable of granulating in one step, the operation is simplified and the production efficiency can be improved.
WO2010059916A3 Preparation of docetaxel The present invention relates to docetaxel and processes for preparing docetaxel, including process-related intermediates. The present invention also relates to processes for preparing substantially pure docetaxel and intermediates.
CN1569010A Etimicin sulfate preparation and its preparing method The invention discloses etimicin sulfate preparation and its preparing method which comprises, charging acids or alkali as pH conditioning agent so as to increase the dissolving degree of the etimicin, charging right amount of isoosmotic adjustment agent, thus resulting the action of quick sterilization.
EP2785203A1 Increasing the bioavailability of hydroxycinnamic acids The present invention generally relates to the field of nutrition, health and wellness. For example, the present invention relates to hydroxycinnamic acids and their health benefits. The present invention discloses compositions that allow increasing the bioavailability and/or bioefficacy of hydroxycinnamic acids. According to the invention, this can be achieved by co-administering at least one glycoside conjugate of a flavonoid with hydroxycinnamic acids.
WO2008043175A1 SOLUBLE β-N-ACETYLGLUCOSAMINIDASE BASED ANTIBIOFILM COMPOSITIONS AND USES THEREOF The present invention provides compositions comprising an antibiofilm enzyme, a soluble β-N- acetylglucosaminidase similar to the dspB gene (DispersinBTM ), and an antimicrobial for preventing growth and proliferation of biofilm-embedded microorganisms in acute and chronic wounds, and methods of treatment. The invention further provides methods for preparing medical devices, and in particular, wound care devices using DispersinB TM-based antimicrobial compositions.
CN102614149A Method for preparing sinomenine capsules The invention provides a method for preparing sinomenine capsules and has the advantages that a displacement method is adopted for preparing sinomenine, the operation is simple, during the extraction process, heating is not needed and cold treatment is adopted; the yield is high, and treatment of mother liquid is simple; and the method is safe and reliable and low-pollution and plays a positive role in environmental protection.
US20100322965 Viral vaccine vectors The present invention relates to a hybrid-viral vector system, in particular, but not exclusively, to a hybrid-viral vector system that can be used as a vaccine vector.
CA2533791C Medicaments for inhalation comprising betamimetics and an anticholinergic agent The present invention relates to novel pharmaceutical compositions based on beta2 agonists and salts of a new anticholinergic, processes for preparing them and their use in the treatment of respiratory complaints, wherein the anticholinergic agent has the formula (I).
CN103690530A Application of ethyl 6-chlorocoumarin-3-carboxylyl L-theanine and the like in preparation of product used for preventing and treating disease such as cancers The invention relates to the field of medical technology. Ethyl 6-chlorocoumarin-3-carboxylyl L-theanine, a novel synthetic compound, can inhibit the growth and invasion of cancer cells of human lung cancer, breast cancer, liver cancer, gastric cancer, colon cancer, prostatic cancer, pancreatic cancer, cervical cancer, lymphadenoma, leucocythemia, melanoma, and the like, and can remarkably inhibit the growth and metastasis of the tumors in a body, with an inhibiting effect exceeding the inhibiting effects of anti-cancer drugs. The mechanism of action involves the down regulation inhibition of the bonding of the receptors which are closely related to growth, invasion and metastasis of the tumors, signal transduction regulation and control proteins, the kinase level and a nuclear factor with DNA, and also upper regulation of factors such as cancer-inhibiting proteins and cell cycle inhibition proteins. The ethyl 6-chlorocoumarin-3-carboxylyl L-theanine can directly inhibit the activity of histone deacetylase, the activity of histonemethylferase EZH2, and combination of a inflammatory factor NF-[Kabba]B and DNA. The activity of the ethyl 6-chlorocoumarin-3-carboxylyl L-theanine exceeds the activity of clinical anti-cancer drugs. The invention provides new applications of the ethyl 6-chlorocoumarin-3-carboxylyl L-theanine in prevention and treatment of diseases such as tumors, inflammation, heart and cerebral vessels and immunodeficiency.
US20100074957 Intraocular formulation Biodegradable therapeutic agent incorporating microspheres formulated in a high viscosity carrier suitable for intraocular administration to treat an ocular condition. The formulation can also be used to treat non-ocular conditions such as articular pathologies.
EP1944025A1 Stable pharmaceutical compositions of orlistat The present invention relates to stable pharmaceutical compositions of orlistat for treatment or prevention of obesity and hyperlipidemia. The pharmaceutical compositions contain Orlistat form I, which does not convert to form II at the temperatures encountered during manufacturing of an orlistat dosage form.
WO2008157211A1 Crystalline forms of (3aalpha,4beta,5alpha,7beta,7aalpha)-4-(octahydro-5-ethylsulfonamido-4,7-dimethyl-1,3-dioxo-4,-7-ep0xy-2h-isoind0l-2-yl)- Crystalline forms of (3aα,4β,5α,7β,7aα)-4-(octahydro-5-ethylsulfonamido-4,7- dimethyl-l,3-dioxo-4,7-epoxy-2H-isoindol-2-yl)-2-(trifluoromethyl)benzonitrile are provided. Also provided are at least one pharmaceutical composition comprising at least one crystalline form of (3aα,4β,5α,7β,7aα)-4-(octahydro-5-ethylsulfonamido- 4,7-dimethyl-l,3-dioxo-4,7-epoxy-2H-isoindol-2-yl)-2-(trifluoromethyl)benzonitrile, and at least one method of using at least one crystalline form of (3aα,4β,5α,7β,7aα)-4- (octahydro-5-ethylsulfonamido-4,7-dimethyl-l,3-dioxo-4,7-epoxy-2H-isoindol-2-yl)- 2-(trifluoromethyl)benzonitrile to treat cancer and/or other proliferative diseases.
US20120045429 Methods and Agent for Modulating the RNA Polymerase II-Histone Surface The present invention relates to the identification of an intranucleosomal DNA loop formed during transcription through a nucleosome and use of the same to identify an agent that modulates the RNA Polymerase II-histone surface.
EP2267029A2 Methods and compositions for treatment of inflammatory disease using Cadherin-11 modulating agents A method for treating inflammatory joint diseases by inhibiting cadherin-11 mediated cellular function using a cadherin-11 modulating agent is provided. Also provided are screening assays for identifying pharmaceutical lead compounds capable of modulating cellular functions of cadherin-11 such as cell proliferation, apoptosis, factor secretion, and binding of cadherin-11 to cadherin-11 counter-receptor inhibiting binding of cadherin-11 to its counter-receptor either in the context of a cell or in soluble form.
US20110082192 Lipoic acid acylated salicylate derivatives and their uses The invention relates to lipoic acid acylated salicylate derivatives; compositions comprising an effective amount of a lipoic acid acylated salicylate derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a lipoic acid acylated salicylate derivative.
US20050065140 Antidepressant; side effect reduction There is provided a selective serotonin reuptake inhibitor having affinity for serotonin 1A receptors which comprises a cyclic amine represented by the formula: wherein G represents a formula (2): a prodrug of said cyclic amine, or a pharmaceutically acceptable salt of said cyclic amine or prodrug, as an active ingredient.
EP1121116B1 Sustained release pharmaceutical composition of fluvastatin The present invention is directed to solid, sustained-release, oral dosage form pharmaceutical compositions which contain therapeutic amounts of a pharmaceutically active agent, hydroxypropyl methyl cellulose and anon-ionic, hydrophilic polymer selected from the group consisting of hydroxyethyl cellulose having a number average molecular weight ranging from 90,000 to 1,300,000, hydroxypropyl cellulose having a number average molecular weight of 370,000 to 1,500,000, and poly(ethylene oxide) having a number average molecular weight ranging from 100,000 to 500,000.
US20110190374 Methods of treating a meiotic kinesin associated disease The invention provides methods of treating a meiotic kinase-associated disease, preferably the meiotic kinase HSET, by administering an inhibitor of the meiotic kinase. Preferably, the disease is associated with the presence of supernumerary centrosomes, such as cancer. Methods of inhibiting the growth of a tumor cell by contacting the cell with an inhibitor of a meiotic kinase, preferably HSET, are also provided. Screening methods for identifying inhibitors of the meiotic kinase HSET are also provided. Methods of selecting subjects for treatment with an inhibitor of a meiotic kinase, such as HSET, are also provided.
WO2008052088A8 Chromane derivatives, synthesis thereof, and intermediates thereto Methods of preparing compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, x, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
CN103027950A Psoriasis rehabilitation liquid The invention discloses a psoriasis rehabilitation liquid, which is an external-use medicine for treating psoriasis. The psoriasis rehabilitation liquid comprises the following components: a garter snake, Chinese azalea flowers, root of fangji, scandent schefflera stems and leaves, spatholobus suberctu, schizophragma integrifolium, asarum, musk, pearl grass, camphor, borneol and wine. The medicines have a synergistic effect, effects of expelling wind-damp, dredging meridians and collaterals, dispelling wind and eliminating dampness, promoting blood circulation to arrest pain and inducing dieresis to detoxify. The psoriasis rehabilitation liquid has a good curative effect and a rapid both symptoms and root causes, and can treat both symptoms and root causes, so that the psoriasis is not easily to reoccur after being treated.
US20110159074 Wipe Article Comprising Lotion Composition Comprising Omega-6 Fatty Acid And Method Of Improving Skin Barrier Function A wipe article comprising a composition comprising omega-6 fatty acid. A method of improving skin barrier function of semi-occluded skin comprising the step of contacting the semi-occluded skin with a wipe comprising an omega-6 fatty acid.
US20100222390 Methods and Compositions for the Intravenous Administration of Compounds Related to Proton Pump Inhibitors Disclosed herein are liquid compositions comprising a therapeutically effective concentration of a prodrug of a sulfonyl-containing proton pump inhibitor, wherein said compositions have a pH of from 3 to 7.3. Solid compositions related thereto are also disclosed. Methods of delivering a proton pump related thereto are also disclosed. Compositions comprising a second therapeutically active agent are also disclosed herein.
CN102755339A Application of iodized lecithin in preparing medicines used for treating bronchitis The invention provides an application of iodized lecithin in preparing medicines used for treating bronchitis. The iodized lecithin is especially suitable for treating children bronchial asthma and asthmatic bronchitis. Iodized lecithin assists in improving the expansion effect of epinephrine upon trachea smooth muscle, and can directly act upon lung fibroblast cells. With iodized lecithin, in-vivo serum IgE level can be reduced, IL-4 chemokine generating hyperthyroidism can be inhibited, and tissue obstacle of eosinophils can be inhibited. As results of pharmacological and toxicological tests, iodized lecithin is an effective bronchitis-treating medicine with accurate efficacy and low toxic and side effect. Iodized lecithin is especially suitable for treating children bronchial asthma and asthmatic bronchitis.
CN101054363A Huperzine A derivative, preparation method and application thereof The patent relates to preparing method of huperzine A derivates 1-8 which includes: p-dimethylamino benzaldehyde-huperzine A acetal imines, 3-ethoxymethyl aldehyde-4-hydroxyphthalic formaldehyde-huperzine A acetal imines, 3,5-dimethoxylbenzaldehyde-ethylidene ether imines, 2,4-dimethoxylbenzaldehyde-huperzine A acetal imines, p-cyano formaldehyde-huperzine A acetal imines, 2-sodium sulfonate benzaldehyde-huperzine A acetal imines, alpha-methylinnamic-huperzine A acetal imines and p-dimethylin cinnamic acid-huperzine A acetal imines, also relates to the medicinal composition which takes above huperzine A derivates as effective ingredient, and the application thereof for preparing medicine for inhibiting acetylcholinesterase activity.
US20120238576 Triazine Derivatives and their Therapeutical Applications The present invention comprises inter alia compounds as shown in formula (I) or a pharmaceutically acceptable salt thereof.
WO2006051413A8 Azabenoxazoles for the treatment of cns disorders The present invention relates to a7 nicotinic receptor agonists of formula I as described herein and to a method for treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal an a7 nicotinic receptor agonist of formula I. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant a7 nicotinic receptor agonist of formula (I).
WO2012080232A1 2-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders The present invention relates to substituted imidazopyrizine compounds of general formual (I): in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
EP2571352A1 Selective hdac inhibitors This disclosure is related to compounds having the structure wherein Ar1, Ar2, R1-R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.
CN1931224A Injection for treating thecal cyst The injection for treating thecal cyst is one kind of local injection with simple usage, low cost and high curative effect. The injection in 10 ml contains Qianglining injection in 3-5 ml, placenta tissue fluid solution in 1-2 ml, and 5 % concentration glucose solution for the rest, where each ml of the Qianglining injection contains glycyrrhizin in 1 mg and each ml of the placenta tissue fluid solution contains placenta tissue fluid in 50 mg. The injection is prepared through mixing the Qianglining injection and the placenta tissue fluid solution and adding 5 % concentration glucose solution.
CN102018696A Skin external preparation containing lidocaine or pharmaceutical salt thereof The invention discloses a skin external preparation containing lidocaine or pharmaceutical salts thereof, which comprises the following components in percentage by weight: 0.5-2 percent of lidocaine or pharmaceutical salts thereof, 25-50 percent of moist-locking resin and 0.75-4 percent of penetration enhancer. The specificity combination of the lidocaine or pharmaceutical salts thereof is carried out on anions which use the moist-locking resins as gel carriers, thus greatly reducing the dosage of the bulk drug lidocaine or pharmaceutical salts thereof used in the preparation during acquisition of the same curative effect, reducing the category and the dosage of auxiliary materials simultaneously, simplifying the operation process and reducing the production cost. The skin external preparation prepared by using the method has the functions of strong drug loading rate, excellent moisture capability, ventilation property and penetrability, obvious curative effect, no sensitization and the like, and is convenient in use.
WO2006097808A1 Benzimidazolone derivatives as cb2 receptor ligands This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis or bronchitis.
CN101006985A Pharmacological composition The invention relates to sustained release formulations comprising 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine or a pharmaceutically acceptable salt thereof, to methods of treating psychotic states and hyperactivity utilizing the sustained release formulations and to a process for preparing the sustained release formulations.
US20120010296 Treating various disorders with catechol-o-methyl-transferase inhibitors The invention provides methods for treating disorders in patients with catechol-o-methyl-transferase inhibitors, such as impulse control disorders and cognitive disorders, such as attention deficit hyperactivity disorder. The invention also provides methods for treating patients with obsessive compulsive disorders and substance addictions with catechol-o-methyl-transferase inhibitors.
CN101693015A Coenzyme A medicament freeze-drying preparation and process for preparing same The invention discloses a coenzyme A medicament freeze-drying preparation, which adopts disodium hydrogen phosphate and sodium dishydrogen phosphate buffered salt liquor to protect a coenzyme A in the process of preparing the freeze-drying preparation. The freeze-drying preparation selects phosphate buffered salt liquor in the process of preparing medical liquor to enable the coenzyme A to be in the liquor with relatively constant pH values. Simultaneously, the phosphate buffered salt liquor is favorable for stabilizing a coenzyme A molecular structure containing phosphate groups, a coenzyme A potency (marked content) is lowered by no more than 2.5% from the process of preparing and filling to the beginning of freeze-drying.
CN103432153A Novel prescription of injection for treating infectious pleuropneumonia of livestock and preparation technology thereof The invention discloses a novel prescription of an injection for treating infectious pleuropneumonia of livestock. The prescription is prepared from the following raw materials by weight: 3 to 7 kg florfenicol, 2 to 4 kg azithromycin, 0.2 kg bromhexine hydrochloride, 2 to 4 ten thousand ml alpha-pyrrolidone, 1 to 3 ten thousand ml dimethylformamide, 2.5 ten thousand ml propylene glycol, 1 ten thousand ml glycerinum and appropriate amount of water for injection. The invention further provides a preparation technology of the novel prescription of the injection for treating infectious pleuropneumonia of livestock, the preparation technology comprises the following steps: dimethylformamide, pyrrolidone and propylene glycol are taken according to the prescription, and put into a liquid mixing jar, and heated to be 70 to 80 DEG C; glycerinum is taken according to the prescription, and added into the liquid mixing jar and stirred to enable the glycerinum to be dissolved completely. The prescription provided by the invention is widely used for treating respiratory diseases and infection caused by sensitive gram-positive bacteria.
DE102004024241A1 Water-soluble starch acetate useful in biomedical, pharmaceutical and food applications, especially as a blood plasma expander Water-soluble starch acetate (I) produced without using enzymes and vinyl acetate, with a molecular weight of 50000-1000000 and a degree of substitution of 0.3-1.2, where 85-100% of the acetyl groups are in the 2 position of the anhydroglucose unit, is new. An independent claim is also included for producing (I) by reaction in an organic solvent.
CN103393685A Pharmaceutical composition containing oxaliplatin and fluorouracil The invention relates to a pharmaceutical composition containing oxaliplatin and fluorouracil, and especially relates to an application product of the pharmaceutical composition, wherein the application product comprises an oxaliplatin injection and an injection containing fluorouracil. Administration comprises following steps, the oxaliplatin injection is dissolved and diluted for independent intravenous drop infusion, and then the fluorouracil injection is dissolved and diluted for intravenous drop infusion, wherein the oxaliplatin injection must be applied to drop infusion before the fluorouracil injection.
US20120046264 Commercial scale production methods for transdermal hormone formulations Methods for commercial production of transdermal formulations comprising a hormone compound are provided. In particular, methods for commercial scale production under an inert atmosphere of a transdermal formulation comprising a therapeutically effective amount of a hormone, preferably a testosterone compound, useful for the treatment of hypoactive sexual desire disorder (HSDD) in postmenopausal women are provided.
WO2013133393A1 Single-stranded nucleic acid molecule for inhibiting vegf gene expression Provided is a new nucleic acid molecule that inhibits the activity of TLR 3 and the expression of the VEGF gene. The single-stranded nucleic acid molecule for inhibiting the expression of the VEGF gene is characterized in that: a 5'-side region (Xc), an internal region (Z) and a 3'-side region (Yc) are included, in that order, from the 5' side to the 3' side; the internal region (Z) is formed by linking an internal 5'-side region (X) and an internal 3'-side region (Y); the 5'-side region (Xc) is complementary to the internal 5'-side region (X); the 3'-side region (Yc) is complementary to the internal 3'-side region (Y); and at least one region among the internal region (Z), the 5'-side region and the 3'-side region includes an expression-inhibiting sequence that inhibits the expression of the VEGF gene. The single-stranded nucleic acid molecule is capable of inhibiting the activity of TLR 3 and the expression of the VEGF gene.
CN101797236A Rivastigmine orally disintegration tablet and preparation method thereof The invention discloses a rivastigmine orally disintegration tablet and a preparation method thereof. The orally disintegration tablet comprises the following components by mass percent: 0.2 to 5 percent of rivastigmine, 60 to 90 percent of filler, 5 to 30 percent of disintegrating agent, 0.1 to 2 percent of lubricant and 0.2 to 5 percent of correctant. The invention has smooth and attractive appearance, proper hardness, quick disintegration in oral cavity, absorption and response, high bioavailability, small thrill on gastrointestinal tract, good taste, convenient administration and is particularly applicable to the Alzheimer disease or Parkinson disease dementia patient who has difficult deglutition or inconvenient drinking problem. The orally disintegration tablet is prepared through a wet granulation wafer method or a powder direct wafer method, has the advantages of simple technology, stable and controllable preparation quality and low cost and is applicable to industrial production.
US20120219621 Composition with Enhanced Thermogenic Activity and the Use Thereof in the Prevention and Treatment of Obesity A composition with enhanced thermogenic activity and the use thereof in the prevention and treatment of obesity Pharmaceutical compositions of a dietary supplement or medical device, useful for the treatment and prevention of overweight and obesity and metabolic syndrome comprising: a) menthol or a peppermint essential oil comprising menthol, in association with one or more components having a thermogenetic activity, selected from: b1) capsaicin or a capsacinoid derived from Capsicum genus or a Capsicum extract containing capsaicin and/or capsacinoids; b2) a sulphur containing active principle derived from the Allium genus or an Allium extract containing it; b3) a catechin active substance derived from the genus Camellia or a Camellia extract containing it. The menthol and mint essential oil have a potentiating action on the biological activities of the other aforementioned components.
WO2014015673A1 4-position substituted pyrazolopyrimidine derivative, and use thereof in drug preparation Provided are a 4-position substituted pyrazolopyrimidine derivative having a structure represented by formula I, and a use thereof in drug preparation. The pyrazolopyrimidine derivative is used for preparing a kinase inhibitor, a drug for treating an autoimmune disease, an angiogenesis inhibitor, and an antitumor drug.
CN102657868A 5-hydroxy tryptamine 2 receptor antagonist or transporter inhibitor for treating fatty liver or hyperlipemia The invention relates to the field of medicine, in particular to usage of a 5-hydroxy tryptamine 2 receptor antagonist or transporter inhibitor for treating fatty liver or hyperlipemia. Pharmacological experiments show that the 5-hydroxy tryptamine 2 receptor antagonist or the transporter inhibitor can effectively treat nonalcoholic fatty liver or dyslipidemia of rats caused by high-fat diet and is expected to be applied to treatment of fatty liver or hyperlipemia clinically.
CN102579452A Preparation method of tryptanthrin compound and new application of tryptanthrin compound in preparing indoleamine-2,3-dioxygenase (IDO) inhibitor The invention relates to a preparation method of tryptanthrin compound and a new application of tryptanthrin compound in preparing indoleamine-2,3-dioxygenase (IDO) inhibitor, in particular to an application of tryptanthrin compound in preparing IDO inhibitor and in preparing medicine for preventing and/or treating diseases having pathological characteristics of tryptophan metabolic disturbance mediated by IDO. The structure of the tryptanthrin compound is shown in formula A, wherein R1 and R2 are respectively and independently selected from hydrogen, nitryl, C1 to C5 alkyl, halogen or piperazinyl. The tryptanthrin compound can be used as an IDO inhibitor with high activity and is used for treating diseases having pathological characteristics of tryptophan metabolic disturbance mediated by IDO such as tumor, cancer, Alzheimer disease, autoimmune disease, cataract, mental block, tristimania, anxiety neurosis, acquired immure deficiency syndrome (AIDS) and other serious diseases, and as a medicinal resource which is very difficult to get, the tryptanthrin compound has good potential on researching and developing new medicine.
US20090203698 Compounds for Enzyme Inhibition Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.
CN1962665A Extraction method of antineoplastic composition bhang flavone A from bhang The invention discloses an extracting method of dolichnin A with excellent antineoplastic activity from hemp, which comprises the following steps: (1) extracting for 2-3 times through alcohol; combining extract; condensing into concrete; (2) adsorbing through large-hole resin; eluting through alcohol; combining approximate component; evaporating alcohol; (3) separating to purify rough extract through high-speed reflux chromatogram; forming solvent system of solid phase and fluid phase through skellysolve B, acetic ester, carbinol and water; filling solid phase in the chromatographic column; rotating column to pump fluid phase in the column; sampling; eluting to obtain high-purity product.
CN101712689A Azepine condensed ring substituted cephalosporin derivative The invention belongs to the technical field of medicines, particularly relating to an azepine condensed ring substituted cephalosporin derivative shown in general formula (I) or pharmaceutically acceptable slat thereof, wherein R1, R2, R3, R4, R5, R6, X and n are defined in the specification. In addition, the invention also provides a preparation method of the compounds, medicine composite containing the compounds, and applications of the compounds in preparing medicaments for treating and/or preventing infectious diseases.
CN102961415A Application of phellinus lonicericola or extract thereof The invention discloses an application of phellinus lonicericola or an extract thereof to the preparation of drugs or healthcare products for regulating estrogens and treating perimenopausal syndrome. The invention also provides a new application of a compound hispolon. The phellinus lonicericola and the extract thereof or the compound hispolon can be combined with estrogen receptors to doubly regulate the estrogens and has the function of promoting the secretion of endogenous estrogens when the endogenous estrogens are insufficient; by using the phellinus lonicericola and the extract thereof or the compound hispolon for treatment, various symptoms and signs can be effectively relieved, the function of slowing down the occurrence and the development of the long-term symptoms such as osteoporosis, cardiovascular disease and the like is provided, the quality of life of the perimenopausal syndrome women can be improved and a new way is developed to treat the perimenopausal syndrome.
US20110020478 Method for treating neural injuries A method for treating neural damage with a composition prepared from roots of bupleurum and scutellaria.
CA2566837A1 Anti acne skincare composition and skincare article There is disclosed a cleansing and moisturising composition for topical application to the skin. The composition comprises salicylic acid as active ingredient, and has the form of an emulsion comprising 70-95% by weight of an aqueous phase and 5-30% by weight of an oil phase, the salicylic acid being dissolved in the oil phase, and the composition comprising one or more moisturising agents. The composition may be incorporated into a wipe substrate for ease of application to the skin. The compositions have the combined effects of cleansing and moisturising the skin and may be used in the prophylactic or remedial treatment of acne.
US20110059926 Vitamin D Compounds and Methods for Reducing Ocular Hypertension (OHT) The present invention relates to compounds and methods for reducing intraocular pressure and treating ocular hypertension in a subject.
US7354946 Biarylurea derivatives The present invention relates to a compound of Formula (I) and the manufacturing method(s) thereof and the use thereof: Formula (I) wherein: Ar is a nitrogen-containing heteroaromatic ring group; X and Z are each a carbon atom, and so on; Y is CO, and so on; R1 is a hydrogen atom, and so on; R2 and R3 are each a hydrogen atom, and so on; R4 and R5 are each a hydrogen atom, and so on; and the formula is a single bond or a double bond. According to the present invention, the compound of the present invention can provide Cdk4 and/or Cdk6 inhibitors for treating malignant tumors, because the compounds of the present invention exhibit a prominent growth inhibitory activity against tumor cells.
US20060100245 Substituted biphenyl-4-carboxylic acid arylamide analogues Substituted biphenyl-4-carboxylic acid arylamide analogues capable of modulating receptor activity, are provided. Such ligands may be used to modulate receptor activity in vivo or in vitro, and are particularly useful in the treatment of pain and other conditions associated with receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for receptor localization studies.
CN102525988A Quetiapine fumarate sustained-release tablets The invention relates to quetiapine fumarate sustained-release tablets. The quetiapine fumarate sustained-release tablets are characterized in that: a regulating layer is arranged outside a sustained-release medicine layer in a tablet core, so the early-stage release rate of the medicine can be controlled, the final-stage residue phenomenon is avoided, release is controlled accurately, the process is simple and cost is low.
WO2008024374A2 Inhibitors of pancreatic phospholipase a2 for altering cholesterol and fat uptake Disclosed herein are methods for regulation of fat and/or cholesterol uptake from the gastrointestinal tract and/or regulation of plasma fat and/or cholesterol levels comprising administering to a mammal in need thereof an effective amount of a regulator of pancreatic IB PLA2 functionality. Also disclosed herein are methods of regulating the function of a polypeptide of interest comprising inserting of the 62-66 loop region of a pancreatic IB PLA2 amino acid sequence into the polypeptide of interest; and administering an effective amount of a regulatory molecule that effects its regulation through said amino acid sequence. Further disclosed are novel bile salt compounds that regulate pancreatic IB PLA2. Methods for detecting altered pancreatic IB PLA2 function and methods for identifying an agent suitable for regulating pancreatic IB PLA2 enzyme functionality are also disclosed.
CN101434660B Method for extracting Ganoderma lucidum polysaccharide by ultrasonic wave-microwave combination The invention relates to a method for ultrasonic-microwave synergistic extraction of ganoderma lucidum polysaccharide. The technology includes the main steps as follows: a fruiting body of a ganoderma lucidum is dried at 50 DEG C to 60 DEG C, crushed and screened by a sieve of 20 to 60 meshes; the screened ganoderma lucidum powder is added into water so as to lead the weight ratio between material and solvent to be 1:20 to 1:50; an ultrasonic-microwave synergistic extractor is used for extraction with ultrasonic wave 50W, microwave 10W to 400W and an extraction period of 10 min to 60 min; after extraction is completed, cooling, centrifugal separation and filtering are carried out in sequence to obtain a supernatant fluid contaning ganoderma lucidum polysaccharide; the supernatant fluid iscondensed to 1/2 to 1/3 of the original volume, added with anhydrous ethanol till the content of ethanol reaching 70 percent to 85 percent in the solvent; the solvent stands till complete deposition at 4 DEG C, and then filtering and vacuum freeze-drying are carried out to obtain the ganoderma lucidum polysaccharide. The method adopts the advantages of microwave and ultrasonic wave, such as even vibration and uniform effect on each point in a sample medium, has more types of selectable extractants and larger scope of target extracts, reduces binding force between a target compound and the sample body, accelerates the process of changing into solvent phase from solid phase of the target compound and has a large amount of sample processing.
WO2009091932A2 Treatment of mild dementia of the alzheimer's disease type Methods, compositions, and kits for slowing progression of Alzheimer's disease symptoms in a patient with mild Alzheimer's disease are described.
US20080014291 Process for the Production of Multi-Component Mineral Substance Preparations Process for producing mineral substance preparations with multiple components that contain a low level of or no contaminants wherein material of plant or animal origin is used and at least two different thermo-oxidative treatment steps in separate locations are carried out. Mineral substance preparations produced according to the invention are characterized in that they basically contain the mineral substances that the respective plant absorbs from the ground in a highly bio-available form, at the same time have a very low content of thermally-modified organic compounds. Not easily dissolvable a priori trace elements are therefore preferably in colloidal form, which is why biologic absorption is especially high. The effect of these mineral substance preparations on health and fitness are by far superior than the currently available mineral substance preparations, since they also all contain trace elements that can no longer be analytically verified but can nevertheless have a considerably energizing effect on the human body.
US20080076798 Injectable dosage form of aqueous solution including a buffer and optional amino acid at alkaline pH; e.g. argatroban, lactobionic acid, and methionine; free of ethanol, saccharides and sugar alcohols; reducing dosage errors, storage stability An aqueous formulation of argatroban and of related compounds is disclosed along with a reconstitutable formulation, each of which is substantially, if not totally alcohol free. The formulations are also substantially free, if not totally free, of mono-, di-, and oligo-saccharides. An especially preferred embodiment is a ready-to-administer 1 mg/ml injectable dosage form having argatroban, lactobionic acid, and methionine.
US7355069 2-[2-(4-{2-[ethyl(2-fluorobenzyl)amino]-2-oxoethoxy}phenyl)ethoxy]benzoic acid; peroxisome proliferator-activated receptors alfa agonist; antidiabetic, hypotensive agent; obesity, elevated VLDL (Very Low Density Lipoproteins) and reduced HDL (High Density Lipoprotein) concentrations The present invention provides a compound of formula (I), wherein n is 0, 1 or 2 and R1 represents halo, a C1-4alkyl group which is optionally substituted by one or more fluoro, a C1-4alkoxy group which is optionally substituted by one or more fluoro and wherein when n is 2 the substituents R1 may be the same or different; R2 represents a C2-8alkyl group which is optionally interrupted by oxygen; Y is absent or represents methylene; and X is O or S; and pharmaceutically acceptable salts and prodrugs thereof, to processes for preparing such compounds, to their utility in treating clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them
US20090035294 Lipopolysaccharide fractions of vitreoscilla filiformis useful for stimulating the synthesis of anti-microbial peptides of the skin Specific fractions of Vitreoscilla filiformis comprising its Lipid A are useful for stimulating the synthesis of anti-microbial peptides of the skin.
EP1874340A2 Elastin protective polyphenolics and methods of using the same Dermal fibroblasts permanently loose their ability to synthesize elastin, the major component of elastic fibers, shortly after puberty. This progressive loss of elastic fibers cannot be replaced, resulting in the physical signs of aging. The present invention provides methods and compositions containing the polyphenols ellagic acid and/or tannic acid for protection against degradation of cutaneous elastic fibers by the elastolytic enzymes. The use of ellagic acid and/or tannic acid increased the overall deposition of elastic fibers in healthy and damaged skin cells. The protection of both intra- tropoelastin and extra-cellular mature elastic fibers from proteolytic enzymes by ellagic acid and tannic acid caused an increase in the net deposition of elastic fibers. Therefore, embodiments of the present invention provide methods and composition for the treatment of skin and prevention and treatment of degradation of dermal elastic fibers.
US6894051 Crystal modification of a N-phenyl-2-pyrimidineamine derivative, processes for its manufacture and its use The invention relates to a new crystalline form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]benzamide of formula 1, which may be used for example for tumor therapy.
US20130045267 Methods of using agents that modulate claudin expression Methods are provided for modulating expression of claudin-1 and/or claudin-23, for purposes of regulating formation of tight junctions in keratinocytes or other types of cells such as antigen presenting cells (e.g., dendritic cells and Langertians cells), by either increasing or decreasing expression of claudin-1 and/or claudin-23. Also provided are transdermal formulations that decrease expression of claudin-1 and/or claudin-23, thereby diminishing tight junction formation in cells expressing claudin-1 and/or claudin-23, as well as a transdermal patch for delivering the same.
CN102755346A Compound polysaccharide formula of edible fungus as well as preparation method and application thereof The invention relates to a compound polysaccharide formula of edible fungus as well as a preparation method and an application thereof. The compound polysaccharide formula comprises the following materials in parts by weight: 50-150 parts of phellinus linteus polysaccharides, 50-150 parts of grifolan and 50-150 parts of hericium erinaceus polysaccharide. The invention is conductive to enhancing the immunologic function of a human body, is anti-tumor, has the action for relieving and treating the diseases such as tumor patients, low resistance, arteriosclerosis, diabetes mellitus and the like and has an obvious effect for calming the nerves of crowds with high mental level and neurasthenia.
CN101189995A Acanthopanax giraldii harms tea The invention relates to a health care tea, which is characterized in that ivy sapogenin, olea acid and Acanthopanax giraldii Harms polysaccharide are mixed proportionally. The ivy sapogenin can be used for resisting hyperlipidemia and inhibiting the absorption of cholesterol. The olea acid has a plurality of pharmacological effects of liver protecting, stomach protecting, heart strengthening, arrhythmia resisting, reducing blood sugan and blood fat, hypertension resisting, inflammation curing, antivirus, immune-regulation, inhibiting platelet aggregation and anti-oxidation, etc, and has little toxic side-effect and high safety. The Acanthopanax giraldii Harms polysaccharide has certain effects on tumor, which can induce tumor cell apoptosis and influence human leukemia cell ultrastructure to death and can inhibit growth, proliferation and colony-forming of tumor cell, the AGP also has immune regulatory function, hematopoietic function and liver protecting effect.
WO2014111871A1 4,5-dihydroisoxazole derivatives as nampt inhibitors The present invention provides substituted 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly NAMPT inhibitors and in which R1 R2, Y, X, "Het" and "p" have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-dihydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salts or stereoisomers or N-oxide thereof.
US20080019955 Surface Protection of Exposed Biological Tissues The invention relates to a biodegradable barrier network comprising at least two polypeptides, one being anionic and the other one cationic. The invention also relates to applicators and kits comprising components to be used to create said biodegradable barrier network. The invention also relates to the use of said applicator or kit in therapy, such as in medicine, veterinary medicine and horticulture.
CN101618019B Triamcinolone acetonide acetate particle, and preparation method and medicinal composition thereof The invention discloses a triamcinolone acetonide acetate particle, and a preparation method and a medicinal composition thereof. The preparation method comprises the following steps: 1) heating and dissolving triamcinolone acetonide acetate with aqueous solution of ethanol, naturally cooling the obtained solution to obtain acicular crystals, washing away the ethanol from the crystals with water for injection, drying the washed crystals, and then adding the crystals into water for injection at a temperature of 0 to 10 DEG C; 2) linearly adding dropwise triamcinolone acetonide acetate solutiondissolved with dimethyl formamide solution into the mixed solution of the water for injection at the temperature of 0 to 10 DEG C obtained in the step 1), simultaneously stirring the mixed solution, keeping the temperature of the mixed solution at 0 to 15 DEG C, and continuing stirring the mixed solution for 1 to 30 minutes to obtain a mixture of water and crystals; and 3) as usual, filtering themixture of the water and the crystals obtained in the step 2) and vacuum-drying the obtained crystals. The invention adopts a crystal inoculation process, thus crystals of the prepared triamcinolone acetonide acetate particles have regular shapes and uniform particle sizes; crystallization is free from jet milling and the physicochemical property of the particle is stable; and no crystal expansion phenomenon generates in the prepared triamcinolone acetonide acetate suspension injection during storage.
CN102429919A Water-soluble vitamin combination medicine The invention provides a water-soluble vitamin combination medicine. The combination medicine is characterized in that: the medicine is prepared according to a medicinal effect component ratio of aneurine hydrochloride: riboflavin riboflavin sodium phosphate: pyridoxine hydrochloride: cobamamide: sodium ascorbate: nicotinamide: folic acid: biotin: sodium pantothenate: glycine: methyl para-hydroxybenzoate: glutathione: disodium edetate of 2.0-4.0:3.0-5.0:3.5-7.0:0.002-0.008:100-150:30-50:0.3-0.7:0.04-0.08:10-20:30-80:0.1-0.4:0.02-0.04:0.2-0.8. The invention also provides a preparation method of the combination medicine. The water-soluble vitamin combination medicine of the invention is better than water-soluble vitamin combination medicines prepared with the prior art in safety, stability and curative effect.
CN103006605A Bendazac lysine sustained release preparation as well as preparation method and application of preparation The invention discloses a bendazac lysine sustained release oral preparation for treating diabetic complications. The sustained release preparation is prepared from bendazac lysine, a hydrophilic gel matrix, a diluting agent, a binding agent, a lubricant/flow aid and a wetting agent according to certain weight proportions. The preparation is a tablet or a capsule; the diabetic complications can be diabetic nephropathy, diabetic neuropathy and diabetic cataract. Compared with the common bendazac lysine tablet, the bendazac lysine sustained release oral preparation has the advantages that the preparation slowly releases and enters into a human body, has small fluctuation of blood concentration 'peak valley', small toxic and side effects and long half-life period, the number of times of taking medicines by patients is reduced and the preparation is safer in use, effective and economic and is an effective ideal medicine for treating the diabetic complications.
US20100291171 Hyaluronic acid derivatives obtained via "click chemistry" crosslinking Crosslinked derivatives of polycarboxylated polysaccharides are described, wherein at least one of the polysaccharide chains consists of hyaluronic acid or a derivative thereof, crosslinked by means of reactions of the “click chemistry” type and their use in the field of viscosupplementation, plastic surgery, oncologic and reconstructive surgery and also as matrices for controlled release systems of biologically and/or pharmacologically active molecules and/or macromolecules.
US20130098797 Two phase pharmaceutical delivery system A bi-phasic pharmaceutical composition for oral administration including one or more solid active ingredient containing particles dispersed within a semi-solid carrier formulation. The solid particles include a coating with pH-triggered drug release properties and the semi-solid carrier formulation is formulated at a pH that is different than the pH at which the active ingredient release properties of the coating are triggered. Also described is a delivery system for delivery of the bi-phasic pharmaceutical composition including the bi-phasic pharmaceutical composition described above and a dispenser pouch formed from flexible laminate sheets. Further, a process for manufacturing the two-phase pharmaceutical delivery system is described including the filling the bi-phasic pharmaceutical composition into flexible dispenser pouches, which allows the patient to squeeze and dispense the contents of the package directly into the oral cavity.
WO2014047150A3 Prevention and treatment of cardiovascular diseases using systems and methods for transdermal nitric oxide delivery The present invention generally relates to compositions and methods for treatment of subjects having or at risk of arteriosclerosis, hypertension, sickle-cell anemia, or other conditions. In some cases, the composition may include nitric oxide. The nitric oxide may be present within a first phase comprising a lecithin, such as phosphatidylcholine. In certain embodiments, the lecithin is present in liposomes, micelles, or other vesicles containing nitric oxide. The composition can take the form of a gel, a cream, a lotion, an ointment, a solution, a solid "stick," etc., that can be rubbed or sprayed onto the skin, e.g., onto a location with acne, or on another suitable portion of the skin. Other aspects of the present invention are generally directed to methods of making or using such compositions, methods of promoting such compositions, kits including such compositions, or the like.
CN1856490A Benzimidazole, benzthiazole and benzoxazole derivatives and their use as lta4h modulators Leukotriene A4 hydrolase (LTA4H) inhibitors of formula I, compositions containing them, and their use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and/or conditions associated with inflammation, wherein X is selected from the group consisting of NR5, O, and S, with R5 being one of the H and CH3; Y is selected from the group consisting of CH2 and O; R4 is selected from the group consisting of H, OCH3, Cl, F, Br, I, OH, NH2, CN, CF3.
US20100209528 Storage-stable aqueous solutions of chlorine dioxide and methods for preparing and using them The present invention is for extremely pure solutions of chlorine dioxide, methods for making such solutions and to compositions and methods for storing, shipping and using such solutions. Generally, the chlorine dioxide solutions of the invention are aqueous solutions containing about 2500 ppm or less of total impurities. The chlorine dioxide solution can be prepared by passing dilute highly pure chlorine gas through a bed of substantially solid sodium chlorite and contacting the resulting chlorine dioxide gas with a liquid.
US20080050452 Metal-containing formulations and methods of use Metal-containing materials, as well as their preparation, formulations, and use are disclosed.
CN102381997A Propofol hydroxy acid ester compound with amino-acid ester constitutional terminal, preparation method for same and application thereof Disclosed are a propofol hydroxy acid ester compound with an amino-acid ester constitutional terminal, a preparation method for the same and application thereof. The propofol hydroxy acid ester compound comprises the constitutional formula (I) or salt formed by HC1 (hydrochloric acid) and CF3COOH (trifluoroacetic acid). Y in the formula refers to a C1-4 linear carbon chain, and R refers to H or CH3 (methyl group). The propofol hydroxy acid ester compound with the amino-acid ester constitutional terminal is capable of reducing first-pass metabolism effect of propofol, and central inhibition can be achieved after orally taking except for an intravenous approach, thereby the propofol hydroxy acid ester compound with the amino-acid ester constitutional terminal can serve as sedate and hypnotic and/or narcotic drugs.
WO2010003369A1 Cyclin-dependent kinases inhibitor of baicalin organic amine derivatives, synthesis and use thereof The present invention provides a cyclin-dependent kinases inhibitor of baicalin organic amine derivatives, synthesis and use thereof. The preparation method is as follows: taking baicalein as lead compound, mixing it with formaldehyde solution and organic amine compounds based on the molar ratio of 1:1-1.2:1-1.2, adding methanol of duplicate weight than baicalein and reacting at 50-70℃; filtering the sediment and washing, and then drying so as to get the product with a content of not less than 97% (weight). Similar to Flavopiridol and P276-00, the activity intensity of baicalein organic amine derivatives inhibiting the cyclin-dependent protein kinase has an increase of about 50 times compared with that of baicalin. It can selectively induce apoptosis of the proliferative phase cancer cells, which has scarcely any influence to the normal structure, and it belongs to anti-tumor drugs of cell cycle inhibitor kind. The product has a rich source of raw materials and also has simple process, high purity, low cost, clear metabolic mechanism, high efficiency and low toxicity, which can be made into oral preparations or injections together with acid salts and is expected to become highly-efficient and low-toxicity anti-tumor and AIDS drugs.
CN1593404A Double layer laminating sustained release tablet of metronidazole and its preparation method Disclosed is a metronidazole double layer laminated slow release tablet comprising two layers, the first layer being a slow release layer consisting of metronidazole, slow release frame, binding agent and lubricating agent, the second layer being a quick release layer consisting of metronidazole, bulking agent, crumbling agent, binding agent and lubricating agent, wherein the mass ratio of metronidazole content in the slow release layer and in the quick release layer is 1 : 0.36-2.75. The invention also discloses the process for preparing the tablet.
US20090304722 Chlamydia trachomatis antigens for vaccine and diagnostic use The present invention is related to antigens from Chlamydia trachomatis which are recognized by specific antibodies from individuals infected with Chlamydia or which can induce T cells from the same individuals to secrete gamma-interferon. The T cell reactive antigens are present in a whole-cell lysate and have apparent molecular weights of 5-12, 16-20, 25-35 and 58-74 kDa as determined by SDS-PAGE. The antigens of the invention are useful in vaccines but also as diagnostic compositions.
US7132449 useful for the therapeutic treatment of Trypanosoma cruzi infection Compounds of general formula (I): wherein R1, R2, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.
WO2008115069A3 Fatty acid esters of glucocorticoids as anti-inflammatory and anti-cancer agents The present invention relates to certain unsaturated fatty acid derivatives of therapeutically active glucocorticoidesfatty acid esters of glucocorticoids as anti-inflammatory and anti-cancer agents and pharmaceutical formulations containing them.
US20110136894 Shortened Alk1 Regulatory Fragment Regulatory elements for controlling expression of transgenes in angiogenic tissue are provided. One embodiment provides an isolated nucleic acid having at least 80%, 85%, 90%, 95%, 97%, 99% or 100% sequence identity to SEQ ID NO:1, or a fragment thereof that causes expression of a transgene in angiogenic tissue. Vectors containing SEQ ID NO:1 and one or more transgenes are also provided. A preferred vector is an adenovirus vector. The transgene can encode a cytotoxin, pro-apoptotic polypeptide, or a therapeutic polypeptide. SEQ ID NO:1 regulates the expression of the transgene such that the transgene is only expressed in angiogenic tissue including, but not limited to arteries feeding ischemic tissues. Methods of using vectors containing SEQ ID NO:1 are also provided.
US8445501 Substituted 7-carboxamido-pyrrolo[3,2-d]pyrimidines The compounds of Formula (I), in which R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
US7517895 Synthetic diazonamides The application discloses novel synthetic compounds, modeled after unique toxins extracted from the marine invertebrate Diazona angulata useful in the treatment abnormal cell mitosis. The application also discloses novel methods for synthesis of these compounds and methods of using these compounds.
US6849648 Phenylene alkyne matrix metalloproteinase inhibitors A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.
US20090186904 Substituted Oxindole Derivatives, Medicaments Containing the Latter and Use Thereof The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
CN102319245A Composition containing repaglinide and metformin hydrochloride and preparation thereof The invention relates to a composition containing repaglinide and metformin hydrochloride and a preparation method thereof, belonging to the technical field of medicines. The composition containing repaglinide and metformin hydrochloride consists of repaglinide, metformin hydrochloride, a filling agent, a disintegrating agent, a bonding agent, a latent solvent and a lubricant, wherein the repaglinide is added into the metformin hydrochloride and auxiliary materials in the form of aqueous solution for wet granulation. The preparation method has the advantages of simple and efficient process, small using quantity of auxiliary materials, capability of solving the problem of poor content uniformity caused by small using amount of the repaglinide and increase in the dissolution rate; and moreover, a preparation has a smaller unit quantity and can be applied to industrial mass production.
US20120251612 Wound Healing Device, Method for Making the Same and Method for Treating a Wound A wound healing device includes a mat of aligned nanofibers of polyaniline, o-aminobenzenesulfonic acid copolymer, polyvinyl alcohol and chitsosan oligossacaride. Method for fabricating the mat and treating wounds are also disclosed.
US20060171881 Compounds with high monoamine transporter affinity Featured compounds have high monoamine transport affinity and are characterized by one of the following two general formulas set out above. The compounds bind selectively or non-selectively to monoamine transporters. The compounds are useful to treat various medical indications including attention deficit hyperactivity disorder (ADHD), Parkinson's disease, cocaine addiction, smoking cessation, weight reduction, obsessive-compulsive disorder, various forms of depression, traumatic brain injury, stroke, and narcolepsy.
CN103356654A Application of Chukrasone A in preparing medicines for treating hemorrhagic fever with renal syndrome The invention discloses a novel use of Chukrasone A in preparing medicines for treating hemorrhagic fever with renal syndrome. The experimental studies of Chukrasone A to hemorrhagic fever with renal syndrome in vivo and in vitro show that the Chukrasone A is low in cytotoxicity, and directly kills cells of hemorrhagic fever with renal syndrome and can remarkably inhibit proliferation of the virus. The Chukrasone A has remarkable protective effect to hamsters infected by the virus, so that the disease time is delayed, the course of disease is prolonged and the death rate is reduced. Therefore, the Chukrasone A is an effective and safe medicine for treating hemorrhagic fever with renal syndrome.
CN102372706A Phthalazinone derivative, its preparation method and application in medicament The invention relates to a phthalazinone derivative, its preparation method and application in medicament, particularly relates to a novel phthalazinone derivative of formula (I), its preparation method, a pharmaceutical composition containing the phthalazinone derivative, and an application of the phthalazinone derivative as a therapeutic agent, especially as a poly(ADP-ribose) polymerase (PARP) inhibitor.
US20080312265 Treatment of Drug-Resistant Tumors A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of drug-resistant tumors and/or for the administration to patients who show polymorphisms in the gene coding for DNA topoisomerase I.
CN101679405A 2-aminopyridine analogs as glucokinase activators Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
US6949522 treating or preventing HIV infection, HBV infection or abnormal cellular proliferation by administering said compounds or the related beta -D and beta -L-2'-halo-4'-thionucleosides The present invention includes compounds and compositions of β-halonucleosides, as well as methods to treat HIV, HBV or abnormal cellular proliferation comprising administering said compounds or compositions.
US20110034452 Triazolium salts as par1 inhibitors, production thereof, and use as medicaments The invention relates to novel compounds of formula I where X, A−, Q1, Q2 Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.
EP1562602A2 Immediate release topical pharmaceutical formulation for enhancement of female sexual desire and responsiveness An immediate release topical pharmaceutical composition is provided which is administrable on an as-needed basis to enhance female sexual desire and responsiveness. The formulation contains a Type III, Type IV, Type V, or nonspecific phosphodiesterase inhibitor as an active agent.
WO2013040447A2 Combination therapy with low dosage strength imiquimod and photodynamic therapy to treat actinic keratosis This disclosure is directed to the use of complementary or combination photodynamic therapy and topical therapy with a lower dosage strength imiquimod formulation for treating actinic keratosis.
CN1785051A Method for preparing sour soymilk contg. micron sugared ginseng and bee-glue etc. for tonifying-Yin and nourishing-stomach A micron-class health-care sour bean milk for nourishing Yin and stomach is prepared from traditional sour bean milk, micron-particles of fibrous ginseng root, chlorophyii ketone sodium salt, hedgehog hydnum, American ginseng, asparagus root, freeze-dried royal jelly, propolis chitosan, isomaltose ketone and oligose through proportional mixing, processing and fermenting. Its advantages are high effect and rich nutrients including vitamins, minerals, etc.
WO2008033934A1 Substituted heteroaryl carboxylic acid derivatives as ptb-1b inhibitors Disclosed are compounds and pharmaceutically acceptable salts of formula (I) : which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-lB (PTP-IB), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
US6897211 Thienodibenzoazulene compounds as tumor necrosis factor inhibitors The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-α) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain.
US20110034454 Morpholino pyrimidine derivatives and their use in therapy A compound of formula (I) or a salt, ester or prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.
US20080261941 Inhibitors of fatty acid amide hydrolase; N-pyridin-3-yl-4-(3-{[5-(trifluoromethyl)pyridin-2-yl]oxy}benzylidene)piperidine-1-carboxamide; elevate brain anandamide levels; pain, urinary incontinence, cognitive disorders, anxiety, depression, sleeping, eating, movement disorders, glaucoma, psoriasis The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.
US20090023775 1-[2-(4-benzyl-4-hydroxy-piperidin-1 -yl )-ethyl]-3-(2-methyl-quinolin- 4-yl)- urea as crystalline sulfate salt The invention relates to 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt and a process for its preparation. Further, the present invention relates to the use of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt alone or in combination with other compounds. Further, the present invention relates to formulations of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt in the preparation of pharmaceutical compositions. The invention also relates to the use of such sulfate salts in formulations as neurohormonal antagonists.
WO2007110438A1 Imidazo [1,2 -b] pyridazines, their processes of preparation and their use as gaba receptor ligands The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.
EP1414416A4 Drug delivery system for zero order, zero order-biphasic, ascending or descending drug delivery The invention is directed to a drug delivery device for controlled release of a drug, comprising a core that has a cylindrical plug embedded therein; and a coating that at least partially surrounds the core. The core is comprised of a drug and excipients. The coating surrounding the core is essentially impermeable to the drug. The cylindrical plug, which is embedded in the core, may be hollow or solid. The drug delivery device enables zero-order drug release profiles as well as more complicated release profiles to be obtained. The invention is also directed to a method of making the drug delivery device.
EP2173730A1 Novel compounds 951: a biphenyloxypropanoic acid as crth2 modulator and intermediates The present invention relates to amide compounds useful as pharmaceuticals for treating respiratory disorders such as asthma, rhinitis and COPD.
US7172892 Exhibit protease activity as a single chain or as an activated two chain form; use of polypeptides to identify compounds that modulate the protease activity thereof and as tumor markers Provided herein are polypeptides designated CVSP14 polypeptides that exhibit protease activity as a single chain or as an activated two chain form. Methods using the polypeptides to identify compounds that modulate the protease activity thereof are provided. The polypeptides also serve as tumor markers.
CN102309488A Itraconazole medicinal composition and preparation method thereof The invention relates to a medicinal composition and a preparation method thereof, wherein the medicinal composition comprises 1 part by weight of itraconazole serving as an active constituent, 0.1-0.5 part by weight of tartaric acid, 0.5-2.0 parts by weight of hydroxypropyl methyl cellulose, and other pharmaceutically acceptable auxiliaries. The itraconazole has low solubility, and by means of the method disclosed by the invention, the dissolving-out effect of the itraconazole which is an insoluble medicament can be enhanced.
CN101433723A PH sensitivity type anticancer prodrug as well as preparation method and application thereof The invention relates to a pH-sensitive anticancer prodrug and a preparation method as well as application thereof, which belongs to the field of medicine and chemical industry. The technical problem to be solved is to provide the pH-sensitive anticancer prodrug, and the anticancer prodrug has highest solubility when the pH value is between 4 and 6, can nearly not be dissolved when the pH value is less than 3 or more than 7, and almost does not release adriamycin during the circulation due to small solubility particularly when circulating in blood (the pH value is approximately equal to 7.4), thereby having small toxic side effect. The pH-sensitive anticancer prodrug is a conjugate obtained by coupling the adriamycin and pectin with a molecular weight of between 71,000 and 400,000 through a chemical bond. The pH-sensitive anticancer prodrug is obtained by the following steps: a pectin aqueous solution and an adriamycin aqueous solution are added with a dehydrating agent to react under the condition that the pH value is between 6 and 8, and then are dialyzed and condensed.
US20070265451 Process for the preparation of oxazolidinones and method of use thereof A process for preparing N-(substituted)-C-(substituted methyl)-oxazolidinones, C-(substituted methyl)-oxazolidinones, and N-(substituted)-C-(substituted methyl)-oxazolidinones, preferably chiral, from optically active C-(protected oxymethyl)-oxazolidinones is described. The process can be used to produce combinatorial libraries of the above substituted oxazolidinones in a two or three step reaction comprising a plurality of reagents differing in numbers of carbons or particular substituted oxazolidinones. A number of substituted oxazolidinones produced using the above process have been discovered to have antimicrobial activity.
US20110201642 Bioactive Compounds The invention relates to bioactive compounds derived from an endophytic Aspergillus sp. fungus strain isolated from a Malaysian medicinal plant Garcinia scortechinii and to compositions which contain one or more of these compounds. In particular, the invention relates to compounds according to formula I; or a pharmaceutically acceptable salt, solvate, hydrate or prodrug derivative thereof, as pure stereoisomers, mixture of isomers, in enol form or tautomeric form. These compounds have utility in, for example, anti-cancer treatments.
US20070275965 CXCR4 modulators The present invention is directed to novel compounds and pharmaceutical compositions that inhibit the binding of the SDF-1 chemokine to the chemokine receptor CXCR4 and/or the binding of the SDF-1 or I-TAC chemokines to the chemokine receptor CCXCKR2 (CXCR7). These compounds are useful in preventing tumor cell proliferation, tumor formation, metastasis, inflammatory diseases, treatment of HIV infectivity, treatment of stem cell differentiation and mobilization disorders, and ocular disorders.
CN102366418A Compound zinc undecylenate triamcinolone acetonide ointment and preparation method thereof The invention discloses a compound zinc undecylenate triamcinolone acetonide ointment and a preparation method thereof. The invention relates to the field of medicine. The compound zinc undecylenate triamcinolone acetonide ointment provided by the invention is composed of zinc undecylenate, undecylenic acid, triamcinolone acetonide acetate, and an emulsion substrate. Compared to existing technologies, the preparation method is advantaged in controllable temperature and simple formula, and the product is advantaged in good characters. With the added triamcinolone acetonide acetate, comprehensive inflammation resisting and allergy resisting effects of the medicine are stronger and more durable. The product and the method are especially suitable for industrial productions.
US8080541 Carbocyclic GlyT-1 receptor antagonists The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
US20120184574 Indole derivatives and methods for antiviral treatment The present invention is directed to compounds and forms and pharmaceutical compositions thereof useful for treating a viral infection, or for affecting viral activity by modulating viral replication.
WO2014016238A1 Compositions for oral administration having a beneficial effect on tendinopathies and ligament injuries Compositions for oral administration having a beneficial effect on tendinopathies and ligament injuries, containing as active ingredients curcumin or a mixture of curcuminoids, catechin extract or epigallocatechin gallate, bromelain, and an agent selected from selenium and manganese, preferably in combination with coenzyme Q10.
US20100260812 Thickened fluid composition comprising chlorine dioxide This invention relates to a stable composition and method of making a thickened fluid composition comprising chlorine dioxide. The stable composition includes a mixture containing a chlorite, an acid source, and a thickener component. At least one of the chlorite, the acid source and the thickener component is in particulate form. In an embodiment, the mixture may be a unitary solid body wherein chlorine dioxide is generated upon interaction with an aqueous medium, such as water. A free halogen source may also be added to the mixture in some cases.
WO2010143803A2 New nicotinamide derivatives with anti-androgen effects, processes of preparing, and antiandrogens comprising the same Provided are novel nicotinamide derivatives and pharmaceutically acceptable salts thereof with anti-androgen effects, preparing processes of the same and antiandrogens containing the same as active ingredients. More particularly, the said nicotinamide derivatives have anti-androgen activity, so that they can be effectively used as a preventive or therapeutic agent for androgen-related diseases such as prostatic disease, androgenic alopecia and acne.
US20100158854 Method for treatment of airway and apparatus and kit for use therewith A method of treating an airway in a mammalian body having a mouth, soft palate, uvula, throat and tongue. An implant-forming material is introduced into at least one of the soft palate and uvula for treating at least one of snoring and sleep apnea. An apparatus and kit are provided.
WO2009018726A1 An antrodia camphorata cyclohexenone compound used for inhibiting hepatitis b virus Antrodia camphorata cyclohexenone compounds which is effective in inhibiting hepatitis B virus, in particular 4-hydroxy-2,3-dimethoxy-6-methy-5 [3,7,11-trimethy-dodeca-2,6,10-trienyl]-cyclohex-2-enone isolated from an extract of Antrodia camphorata. Said Antrodia camphorata cyclohexenone compounds of the present invention are cytotoxic to human liver cancer cell strain HepG22.2.15 which are capable of excreting hepatitis B virus, decreasing the production of hepatitis B virus granules, and inhibiting hepatitis B surface antigen (HbsAg) and hepatitis B e antigen (HbeAg), thus to achieve the aim of inhibiting hepatitis B virus.
WO2013064818A1 Aptamers A nucleic acid aptamer comprising the nucleotide sequence shown herein as SEQ ID No. 5, 6, 7, 8, 9, 10, 1, 2, 3 or 4 or a fragment thereof or a sequence which is at least 80% identical therewith and use of nucleic aptamers to detect the presence of pathogenic bacteria in a sample, particularly in a complex matrix - such as a food system.
WO2005007154A1 Preventive and/or therapeutic agent for pain A preventive and/or therapeutic agent for pains which contains as an active ingredient either a tricyclic compound represented by the formula (I): (I) (wherein R1 represents hydrogen, halogeno, (un)substituted lower alkyl, or (un)substituted lower alkoxy; X1-X2-X3 represents CR5=CR6-CR7=CR8 (wherein R5, R6, R7, and R8 are the same or different and each represents hydrogen, (un)substituted lower alkyl, etc.), etc.; Y represents -CH2S-, -CH2SO-, -CH2SO2-, -CH2O-, -CH=CH-, -(CH2)p- (wherein p is an integer of 0 to 2), -SCH2-, -SOCH2-, -SO2CH2-, or -OCH2-; and R2 represents hydrogen, (un)substituted lower alkyl, etc.) or a pharmacologically acceptable salt thereof.
WO2009140469A3 Dosage regimen comprising ap02l/trail, anti-vegf / anti-cd20 and chemotherapy to treat nsclc or non-hodgkin's lymphoma, respectively The invention provides methods of treating non-small cell lung cancer (NSCLC) and non-hodgkin's lymphoma (NHL). The methods include treating cancer cells with an effective amount of Apo2L/TRAIL and selected chemotherapy regimines and antibody therapies. Articles of manufacture and kits comprising Apo2L/TRAIL and package inserts that provide, eg, administration and dosing information for treating cancers such as NSCLC and NHL are also included.
US7960437 Improving aesthetic appearance of skin by reducing wrinkles and fine lines, improving smoothness, texture, firmness, moisture, elasticity and resilience; topical application of a mixture of a phtyol and a cyclic-AMP derivative There are disclosed skin treatment compositions containing cell signaling compounds, which induce and promote the biosynthesis and/or bioactivity of endogenous chemicals that mediate cell to cell communication in the skin between keratinocytes, fibroblasts and other cell types present in the skin. The cell signaling compound is selected from the group consisting of: andrographolide and its derivatives; adenosine cyclic phosphate and its derivatives; hydrolyzed milk proteins; sunflower seed extract; plankton extract; phytol and its derivatives; and mixtures thereof.
US7655651 Biphenyl-4-carboxylic acid (4-chloro-3-{7-[4-(2-diethylamino-ethoxy)-phenylamino]-1-methyl-2-oxo-1,4-dihydro-2H-pyrimido[4,5-d]pyrimidin-3-yl}-phenyl)-amide; protein kinase inhibitors The present invention relates to novel amide derivatives of 3-phenyl dihydropyrimido[4,5-d]pyrimidinones, to a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. The present derivatives are new compounds of the general formula (I).
WO2009148348A1 Method for controlling infections and tumoral diseases by suppressing multidrug resistance The invention relates to biology and pharmacology, in particular to a method for controlling certain pathologies, including infections and tumoral diseases, by means of a new method for suppressing multidrug resistance by using amiodarone or compounds similar thereto. Said multidrug resistance is a substantial pathologic factor of a great number of diseases, including parasitic infections and cancer.
WO2012027543A1 Solid state forms of dabigatran etexilate, dabigatran etexilate mesylate and processes for preparation thereof Crystalline forms of Dabigatran Etexilate and Dabigatran Etexilate mesylate are described in the present application and processes for preparing the crystalline forms. The present invention also includes pharmaceutical compositions of such crystalline forms of Dabigatran Etexilate and Dabigatran Etexilate mesylate, methods of their preparation and the use of such crystalline forms in the treatment of a patient in need thereof.
WO2006021893A3 Pharmaceutical compositions comprising inhibitors of iron transport, and method of identifying iron transport inhibitors, fn staphylococcus aureus Pharmaceutical compositions comprising inhibitors of the SirABC or FhuC iron-siderophore transport system, and their use for treating an infection of Staphylococcus aureus in a subject Screening methods for mdentifymg SirABC or FhuC iron-siderophore transport system inhibitors are also disclosed
EP2397159A2 Combination of morphinan compounds and antidepressant for the treatment of intractable and chronic pain Provided herein are compositions comprising a dextromethorphan analog according to Formula I or Formula II or a pharmaceutically acceptable salt of either of the foregoing and a co-agent, eg., an antidepressant such as a serotonin norepinephrine reuptake inhibitor; a serotonin noradrenaline dopamine reuptake inhibitor; a norepinephrine dopamine reuptake inhibitor; a monoamine oxidase inhibitor; a selective serotonin, reuptake inhibitor; and a tricyclic antidepressant or a pharmaceutically acceptable salt of any of the foregoing. The compositions are useful in the the treatment of pseudobulbar affect, neuropathic pain, neurodegenerative diseases, brain injuries, and the like.
US20110142889 Compositions and methods for oral drug delivery The invention provides a pharmaceutical composition for oral drug delivery comprising a solid dosage form containing an effective amount of a therapeutic agent, a permeation enhancer and a pharmaceutically acceptable excipient and a bioadhesive layer containing a bioadhesive polymer, and optionally comprising an impermeable or semi-permeable layer having an opening capable of directing a unidirectional release of the therapeutic agent and the permeation enhancer from the solid dosage form. Methods of making and using the present pharmaceutical composition are also provided.
CN101428146A Process for producing composite injection formulation for treating esophagus cancer The invention provides a method for preparing a compounded injection preparation for treating esophagus cancer. The method comprises the following steps: taking raw plasma out from a blood bank according to different blood groups; extracting low density lipoproteins from the raw plasma through the centrifugation and density adjustment treatment; preparing and obtaining targeting drug vectors by the purification of the low density lipoproteins; then compounding the targeting drug vectors with aclacinomycin targeting drugs which are used for treating cancer; and injecting the compounded low density lipoprotein-aclacinomycin drugs into a patient matched with the blood group of drug raw plasma to achieve the purpose of esophagus cancer treatment. The clinical practices prove that the low density lipoprotein-aclacinomycin compounded injection preparation achieves satisfactory curative effects in clinical esophagus cancer treatment without obvious toxic and side effects of chemotherapy, is used for treating 252 esophagus cancer sufferers with the effective rate reaching 100% and the survival rate above 96%, and has good values of popularization and utilization.
US20100249162 Process for the introduction of hydroxyethoxy side chain in bosentan The present invention relates to an improved process for the preparation of bosentan. In particular it relates to a process for preparing bosentan substantially free from the dimer impurity of formula (II) and the 6-hydroxy impurity of formula (III). The invention also relates to a pharmaceutical composition comprising bosentan and its use in the treatment of endothelin-receptor mediated disorders.
CN102198085B Triblock copolymer loaded taxane medicaments micelle and freeze-drying preparation, and preparation method and application thereof The invention belongs to the technical fields of medicament forms and preparation of nano medicaments, and relates to a triblock copolymer micelle and freeze-drying preparation loading taxane medicaments, and a preparation method and application thereof. In order to enable the micelle provided by the invention to be used clinically, the loading capacity, entrapment rate and stability of the preparation need to be guaranteed. The micelle is prepared from the following components in parts by weight: 1 part of taxane medicament and 1.5-99 parts of triblock copolymer polycaprolactone-polyethyleneglycol-polycaprolactone, wherein the molecular weight ratio of polycaprolactone to polyethylene glycol in the triblock copolymer is 0.5-3. The micelle or freeze-drying preparation loading taxane medicaments can be used for treating patients with cancer, tumors, Kaposi sarcoma, malignant tumors, tissue dysfunction or hyperplasia secondary to tissue damage and any other disease capable of reacting with the taxane medicaments, and has especially obvious curative effects on hepatoma, liver metastasis, ovarian cancer and breast cancer.
CN101270140A Common camellia flavone glycosides B with estrogen liveness, preparation method and application thereof The present invention provides camellia flavonoid glycoside B with estrogenic activity, a preparation method and applications thereof. The compound is a novel compound prepared from camellia semiserrata Chi seed oil meal, the system of which is named as kaempferol-3-O-Beta-D-glucosyl-(6.1)-2'', 4''-O-diacetyl-Alpha-L-rhamanopyranosyl-(3.1)-3'', 4''-O-diacetyl-Alpha-L-rhamnoside. The compound has obvious estrogenic activity.
CN101011369A Colon-specific ornidazole tablet The invention discloses an Ornidazole colon-positioning enteric coated tablet, which comprises a core and a dressing layer, the core comprises Ornidazole 10-90 wt%, diluted adjuvant 2-70 wt%, disintegrating adjuvant 1-20 wt%, adhereing adjuvant 1-20 wt% and and lubricating agent 0.1-5 wt%.
EP0799032B1 Pharmacologic management of snoring A method of pharmaceutically managing snoring is provided by the instillation intranasally of a solution containing 1-20 % methylsulfonylmethane by weight dissolved in water so as to saturate the nasal mucous membranes. Preferably, the solution has between 10 %-16 % by weight methylsulfonylmethane. The solution may be buffered, and/or a mild analgesic may be included. The method prefers that instillation occur as close to the sleep event as possible, and it should be at least within one hour before a person retires for sleep. The solution may be introduced by spray or drop-wise, and a product packaging the solution in a suitable container is described.
CN101269070A Oral preparation containing amoxicillin, preparation method and application thereof The invention relates to a buccal tablet containing amoxicillin, the preparation method and the use. The invention aims to provide a buccal tablet with amoxicillin adopted as the medicinal ingredient. The buccal tablet can be dissolved among the salvia in the oral cavity and enter the oral cavity, the pharynx and pharyngeal tonsils to play the role of resisting bacteria. The invention adopts amoxicillin and salt derivatives as medicinal ingredients and can be made into various pharmaceutical formulations, such as buccal tablets, candies, dropping pills and so on. The buccal tablet containing amoxicillin has the characteristics of fast effect, excellent curative effect and convenient drug delivery, can directly improve the concentration of antibiotic drugs at the pathological part and enhance the antibacterial capacity of the pathological part, and is more suitable for majorities of patients.
US20080194552 Aminopyrimidine Derivatives With Tie2 Inhibiting Activity The invention relates to a compound of the Formula I or salt thereof wherein Rx, Ry, Rx, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm blooded animal. The invention also relates to processes for the preparation of said compounds.
EP1470113B1 Pyrimidinone viral polymerase inhibitors A class of pyrimidinone derivatives of formula (I): wherein Z, R1, R2 and R3 are as defined herein; and pharmaceutically acceptable salts thereof; are inhibitors of viral polymerases, especially the hepatitis C virus (HCV) polymerase enzyme.
CN102988662A Preparation method of oxytocic powder The invention relates to a preparation method of an oxytocic powder, which comprises the following steps: drying Chinese angelica, Ligusticum wallichii and the like, baking and grinding Crinis carbonisatus and tortoise shell into fine powder, decocting vinegar to boiling and then adding minced drug, and uniformly stirring to pills for eating. The oxytocic powder has the oxytocic effect, and has obvious curative effect on unopened ischium of parturients, or prevention and control of complication.
CN102477001A Benzamide histone deacetylase inhibitor The invention provides a benzamide histone deacetylase inhibitor. The compound is a compound with a structure as shown in the formula (I) or its stereoisomer, enantiomer, diastereomer, hydrate or salt. The invention also relates to a preparation method of the compound, a pharmaceutical composition comprising the compound and an application thereof. The compound has differentiation and antiproliferative activity, and has a good curative effect for treating diseases caused by abnormal gene expression.
CN101143213A Male analeptic and preparing process thereof The invention provides an analeptic for men and the preparation method of the analeptic. 92.5 to 99.5 grams of pine needle extracts, 0.25 to 2.5 grams of SOD with enzyme activity of 3000mu/mg and 0.25 to 5.0 grams of tadalafil are completely mixed uniformly to be filled as a number O capsule and be filled in a special bottle for drug according to the quantity to be the finished product. When the drug is taken orally, the drug is capable of dredging blood vessels, improving blood circulation, reinforcing the SOD, removing the excessive harmful free radical inside human body, improving NO-CG MP signal access regulation and control of a penis cavernous body and reinforcing the male function. Compared with the prior analeptic, the invention is more effective and has the characteristics of acting fast and no toxic and side effect; the invention can be taken by feeding warm boiled water or along with meal soup, which is convenient for being taken.
CN101313903A Medicament composition containing escitalopram The invention relates to a medicine composition containing escitalopram, which comprises granules consisting of the escitalopram or other medicinal salts and disintegrants, and granules consisting of co-dried mannitol and microcrystalline cellulose, and simultaneously comprises sodium chloride. The composition conceals the strong bitterness of the escitalopram, and is used for treating the tristimania.
US8715632 Compositions and methods for the protection of hair from treated pool water Compositions for treating hair are disclosed. Methods of making and using compositions for treating hair are also disclosed.
EP0866656B1 Use of n-substituted pyridones as tumor necrosis factor alpha inhibitors In a preferred embodiment, a method for the inhibition of the synthesis and release of tumor necrosis factor from various cells, comprising: administering to a human or other mammal an effective dose of one or more pharmaceutical substances selected from the group consisting of N-substituted 2(1H) pyridones, N-substituted 3(1H) pyridones, and pharmaceutically acceptable salts thereof.
EP1676576A1 Combinations comprising camptothecin and their use for the treatment of neoplastic diseases A method for treating diseases comprises delivering to a patient in need of treatment a therapeutically effective amount of 20(S)-camptothecin, an analog of 20(S)-camptothecin, or a derivative of 20(S)-camptothecin in combination with an effective amount of at least one of an alkylating agent, epidophyllotoxin, antimetabolite, antibiotic or vinca alkaloid.
WO2008126756A9 Seleniferous compound and, containing the same, plant and nutritional supplement Highly useful novel seleniferous compound and, containing the same, plants and nutritional supplements. There are provided a selenohomolanthionine of the following formula (1), its esters and salts thereof.
CN103705488A Preparation method of sulforaphane capsule The invention relates to a preparation method of a sulforaphane capsule. The method comprises the following steps: (1) dehydrating, drying and smashing a flowering branch of an edible part of fresh broccoli to obtain broccoli dry powder; (2) smashing new harvested mustard seeds, adding distilled water, and carrying out ultrasonic oscillation and suction filtration to obtain crude enzyme; (3) uniformly mixing the broccoli dry powder with the crude enzyme, carrying out enzymolysis and drying to obtain dry broccoli dry powder; (4) adding ethyl alcohol to the broccoli dry powder, carrying out ultrasonic oscillation extraction, sieving and suction filtration to obtain sulforaphane crude extract; (5) concentrating the sulforaphane crude extract to obtain sulforaphane aqueous solution; (6) diluting the sulforaphane aqueous solution to obtain the sulforaphane aqueous solution with the sulforaphane content of 3-5mg/mL; (7) adding the sulforaphane aqueous solution to the dry broccoli powder, and drying after uniform mixing to obtain redried broccoli powder; (8) smashing the redried broccoli powder for capsule filling to obtain the sulforaphane capsule with the sulforaphane content of 6-14mg/g. The preparation method is simple to operate and low in cost.
CN103461996A Toxin expelling, oxygenation and healthcare element capsule The invention relates to a toxin expelling, oxygenation and healthcare element capsule, and belongs to the technical field of trace element healthcare product production. The capsule comprises macro and trace element group vitamin family nanopowder, natural super-active anti-oxidative free radical removal mixed nanopowder, selenium-and-germanium-rich antagonistic adsorption ion exchange mineral element series mixed nanopowder, and toxin expelling and oxygenation fruit and vegetable series extract polyketide synthase ferment mixed nanopowder. Air, foods and water at everywhere are polluted, and everybody has standard exceeding heavy metals, grease and acidic substances, so the multiple cavities, strong antagonistic absorption capability and good catalytic ion exchange performance of natural ore substances are utilized to provide the toxin expelling, oxygenation, disease prevention and disease treatment healthcare element capsule for removing free radicals, heavy metals and toxins and containing natural fruit, vegetable, pine needle extract, polyketide synthase ferment, selenium and germanium in order to effectively dispel toxins from the body and overcome the unbalance of elements in the body.
US20080021001 Methods For Treating Arthritic Conditions In Dogs The present invention relates to a method for eliciting a disease modifying effect on an arthritic condition in a hip or stifle of a canine which comprises administering to the canine a therapeutically effective amount of a bisphosphonate. The present invention also relates to method for eliciting a disease modifying effect on hip dysplasia or stifle instability, the pain associated with hip dysplasia or stifle instability, joint swelling, shallowing of the acetabulum, narrowing of the joint space, subchondral bone sclerosis, preventing osteophyte formation and preventing joint destruction in a canine which comprises administering to the canine a therapeutically effective amount of a bisphosphonate.
US20100260688 New Formulation and Use Thereof Provided are liquid pharmaceutical formulations comprising nicotine in any form for administration essentially to the lungs being acidified and/or alkalized by buffering and/or pH regulation providing for a tmax of nicotine in arterial blood of a subject within a short period of time after administration. The administration is preferably accomplished by spraying an aerosol into the oral cavity for further distribution essentially into the lungs. Methods for manufacturing the formulation is also disclosed, as are uses of the formulation in therapy, such as therapy for treating addiction to tobacco.
US20090023666 Modulators of Hypoxia Inducible Factor-1 and Related Uses The invention features compounds of formulas I or II: and pharmaceutically acceptable salts and prodrugs thereof, as well methods for modulating the effects of local and systemic hypoxic events using the compounds.
EP1962857A2 Use of anecortave acetate as an adjunct during filtration bleb surgery Methods for controlling ocular hypertension by administering anecortave acetate at the site of filtering bleb surgery are disclosed.
CN102488903A Application of miR-224 to preparation of medicament for treating non-small cell lung cancer The invention belongs to the field of gene engineering and especially relates to application of miR-224 to preparation of medicament for treating non-small cell lung cancer. Change of expression of miR-224 generates influences on apoptosis, propagation and drug susceptibility of non-small cell lung cancer cells, so as to illustrate that inhibition of expression of miR-224 can promote apoptosis of the non-small cell lung cancer cells, inhibit propagation of the cells and enhance sensitivity of the cells to chemotherapeutics.
US20110021614 Use of silymarin and silybin in the treatment of neural injury The present invention provides a method of treating neural injury, e.g., spinal cord injury (SCI), or enhancing recovery from the neural injury with silymarin or silybin.
CN103333084A 3,3'-azobis[6-(butanoyloxy)benzoic acid] and preparation method and application thereof The invention discloses 3,3'-azobis[6-(butanoyloxy)benzoic acid] and a preparation method and application thereof. The method comprises the following steps of: synthesizing a symmetric compound 1,3-dibutanoyloxy-2-carbonyl propane by taking 1,3-dihydroxy acetone as a synthesis raw material, and reducing the 1,3-dibutanoyloxy-2-carbonyl propane into dibutyrate 1,3-dibutanoyloxy-2-carbonyl propane; and carrying out an ester condensation reaction between dibutyrate 1,3-dibutanoyloxy-2-carbonyl propane and 1,3-dibutanoyloxy-2-carbonyl propane in the presence of EDCI serving as a dehydrating agent and DMAP serving as a catalyst to generate the target compound 3,3'-azobis[6-(butanoyloxy)benzoic acid]. After being orally taken into colon, 3,3'-azobis[6-(butanoyloxy)benzoic acid] is decomposed to release 5-aminosalicylic acid which acts together with butyric acid on the colon focus to realize a treatment effect.
US20090111770 Pharmaceutical Composition Free From Dexpanthenol, Calcium Ions, and Phosphate and Use of Calcium Chelating Agent and Ophthalmologically Compatible Viscosity Regulator The invention relates to a pharmaceutical composition free from dexpanthenol, calcium ions and phosphate, comprising at least one calcium chelating agent and at least one opthalmologically compatible viscosity regulator and optionally one or more pharmaceutical excipients. The invention further relates to the use of a calcium chelating agent and an opthalmologically compatible viscosity regulator for the production of a phosphate-free pharmaceutical composition for the treatment and/or prevention of epithelial defects.
US20100098682 Effect of Bri Proteins on Ass Production Provided are methods for reducing inhibiting or preventing Aβ and/or AID production by a cell and methods of treating a subject having Alzheimer's disease. Also provided are methods of determining whether a compound is a mimic of a BRI2 or a BRI3. Additionally provided are pharmaceutical compositions of BRI2, BRI3 or furin, or vectors encoding those proteins.
WO2014157918A1 Pharmaceutical composition for inhibiting immune response through inducing differentiation into regulator t cells and promoting proliferation of regulator t cells The present invention relates to new medical use of (tetrahydropyran-4-yl)-[2-phenyl-5-(1,1-dioxo-thiomorpholine-4-yl)methyl-1H-indol-7-yl]amine, and more particularly, to a pharmaceutical composition containing the compound as an active ingredient, which is used for inhibiting an immune response, and/or for inducing differentiation into regulator T cells from undifferentiated T cells and/or promoting proliferation of regulator T cells.
US20050192343 Nerve growth factor activity potentiating agents Agents potentiating nerve growth factor activity are provided for treating Alzheimer's disease which contain as the active ingredient dodecatrienoic acid derivatives represented by the general formula (I): wherein X represents hydrogen, CHO, COOH, COOR (wherein R represents an ester residue or an addition salt comprising an alkali metal salt or an organic acid salt group), provided that in case where X is COOH, it is bonded to the carbon atom at the position marked with * so as to form a lactam O═C—O—.
US20100104628 method of treating neuroblastoma The present invention relates, in general, to neuroblastoma and, in particular, to a method of treating neuroblastoma tumors, including refractory neuroblastoma tumors. The invention also relates to compounds and compositions suitable for use in such a method.
EP1966155A1 Tosylate salt of 6- (4-br0m0-2-chl0r0phenylamin0) -7-fluoro-n- (2-hydroxyethoxy) -3-methyl-3h-benzimi dazole- 5 - carboxamide , mek inhibitor useful in the treatment of cancer The present invention relates to a tosylate salt of Compound 1 t and polymorphs thereof, in particular crystalline and amorphous forms of Compound 1 tosylate salt, and methods of preparation thereof. Pharmaceutical compositions containing these salts as active ingredient, their use in the manufacture of medicaments for use in the treatment and/or prophylaxis of proliferative disease states, such as cancer, in the human or animal body, and their use in methods for the treatment and/or prophylaxis of proliferative disease states, such as cancer, in the human or animal body are also described.
US8029772 Free-flowing anionic surfactant, alkanolamide and electrolytemixture A free-flowing surfactant composition comprising at least one anionic surface-active agent, an alkanolamide, an electrolyte, and water is described. In particular, the composition is a surfactant composition that has free-flowing non-Newtonian shear thinning properties and the ability to suspend components and is stable under at least one freeze/thaw cycle.
CN201727759U Pravastatin sodium enteric-coated capsule The utility model relates to a pravastatin sodium enteric-coated capsule, which comprises an enteric-coated membrane material layer and pharmaceutical preparation filled in the enteric-coated membrane material layer. The utility model overcomes the nausea, vomiting and other adverse reactions caused by the chronic use pravastatin with low bioavailability under gastric acid environment. The pravastatin sodium enteric-coated capsule of the utility model has obvious bioavailability in small intestine alkaline environment, which is better than that in gastric acid environment, and greatly reduces the side effect.
WO2014006867A1 Composition containing biologically active substance The purpose of the present invention is to provide a composition containing a biologically active substance, which has good moldability to such an extent that a satisfactory granular preparation can be prepared therefrom without the need of cutting using a water-cooled cutter, and which can fulfill the performance required for a lumen-bypassing preparation or the like. The composition containing a biologically active substance according to the present invention comprises: 10 to 50 mass% of a protecting substance which comprises (1a) a linear or branched saturated or unsaturated aliphatic monocarboxylic acid having a melting point of lower than 50˚C and having 8 to 24 carbon atoms, (1b) a linear or branched saturated or unsaturated aliphatic monocarboxylic acid having a melting point of 50˚C or higher and having 8 to 24 carbon atoms and (2) a calcium salt of a linear or branched saturated or unsaturated aliphatic monocarboxylic acid, which has a calcium content of 8 to 12 mass% and having 12 to 24 carbon atoms; and 50 to 90 mass% of the biologically active substance which is dispersed in the protecting substance.
US20080249083 isolated nucleic acids coding for novel glutaminyl-peptide cyclotransferase-like proteins (QPCTLs); isoenzymes; useful for the discovery of new therapeutic agents, for measuring cyclase activity; Alzheimer's disease, Familial British Dementia, Familial Danish Dementia, Down Syndrome, Huntington's disease Novel glutaminyl-peptide cyclotransferase-like proteins (QPCTLs), which are isoenzymes of glutaminyl cyclase (QC, EC 2.3.2.5), and to isolated nucleic acids coding for these isoenzymes, all of which are useful for the discovery of new therapeutic agents, for measuring cyclase activity, and for determining the inhibitory activity of compounds against these glutaminyl cyclase isoenzymes.
US20120121704 Aliphatic Amine Polymer Salts for Tableting The tablets, compositions and methods of the present invention, comprising a carbonate salt of an aliphatic amine polymer and s monovalent anion can prevent or ameliorate acidosis, in particular acidosis in patients with renal disease. The tablets and compositions of the present invention maintain a disintegration time of no greater than 30 minutes at 37° C. and at pH of at least 1 for a period of at least ten weeks at 60° C. Furthermore, the tablets are stable for extended periods of time without the need for specialized storage conditions.
CN102988298A Preparation method of sitafloxacin hydrate granule composition The invention relates to a preparation method of a sitafloxacin hydrate granule composition, belonging to the technical field of Western medicine prepration. The sitafloxacin hydrate granule composition is formed by a base tablet and a coating, and is prepared into a sitafloxacin hydrate inclusion compound by adopting carrageenan. The sitafloxacin hydrate granule composition does not have bitter taste.
WO2012041814A1 Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
US20050080137 Laxative preparation The invention relates to L-arginine, a derivative thereof or a pharmaceutically acceptable salt thereof for use as a laxative, for treatment of constipation and for clearing the rectum and/or the colon of a mammal. Compositions suitable for topical administration to an area of the gastrointestinal tract are provided. Orally administered preparations comprising for example an enteric coating that dissolves at a desired location in the gastrointestinal tract; a controlled release formulation; a sustained release formulation; a targeted drug delivery system; or a combination thereof are also provided.
CN101200427A Compounds and method for preparing same The present invention discloses a compound and the preparation method. The compound is 6,9-heptadecene acid-3-linoleoyl-rac-glycerol. The compound can be prepared by fermenting Nodulisporium Xiahanensis nov.Xia (with preservation number CCTCCNO:M207137). The preparation method has the advantages of low cost and high purity of achieved target compound.
EP1294922B1 Treating cancer using organelle crystallizing agents This invention provides a method for visualizing cellular organelles using cellular organelle and/or cytoskeleton crystallizing agents (e.g. tetrazolium violet), a method for isolating cellular organelles using cellular organelle and/or cytoskeleton crystallizing agents, a method for detecting dehydrogenase inhibitors using cellular organelle and/or cytoskeleton crystallizing agents, a method for treating cancer in mammals through cellular-organelle-crystallization-induced-death (herein defined as 'Cocid'), a method for treating cancer using Cocid inducing agents, pharmaceutical compositions containing a therapeutically effective amount of cocid inducing agents, and compositions containing Cocid inducing agents in combination with a pharmaceutically acceptable carrier, diluent or excipient. Said Cocid inducing agents with or without a pharmaceutically acceptable carrier, diluent or excipient, are used in combination with surgery and/or non-surgical anti-tumor treatments.
WO2013190298A1 2h-imidazol-4-amine compounds and their use as bace inhibitors 2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Αβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration methods of therapy, and pharmaceutical compositions containing such compounds. Formula (I) wherein A is -O- or -CH2-, n is 1 or 1.
CN103446131A Application of Lycojaponicumin B in liver fibroblast proliferation inhibiting drug The invention discloses application of Lycojaponicumin B in preparation of a liver fibroblast proliferation inhibiting drug. A pharmacological test proves that the Lycojaponicumin B can obviously inhabit occurrence and development of liver fibrosis and can be used for preparation of drugs for inhabiting the liver fibrosis and preventing and curing liver cirrhosis. The application of the Lycojaponicumin B in the preparation of the liver fibroblast proliferation inhibiting drug is disclosed for the first time. Due to the fact that the skeleton type is a novel skeleton type and the high liver fibroblast proliferation inhibiting activity of the Lycojaponicumin B is previously unimagined, the possibility that other compounds give any revelation does not exist, and the Lycojaponicumin B has outstanding substantive characteristics and meanwhile has a remarkable improvement in liver fibroblast proliferation inhibition obviously.
WO2007099423A1 1-pyrrolidine indane derivatives as histamine-3 receptor antagonists The invention is directed to compounds of the formula (I) as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula (I), a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the Gl tract, hyper and hypo motility of the gastrointestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above.
CN101759680A Kudzu-vine root daidzein-7, 4'-dioxo acetic acid compound and preparation method thereof The invention belongs to the field of medical technology and relates to a kudzu-vine root daidzein-7, 4'-dioxo acetic acid compound and a preparation method thereof; the compound has the following formula, wherein R1 and R2 can be the same of different and are chosen from H, metal ions, organic cations, basic amino acid cations, C1-C10 alkyl group independently; R3 and R4 can be the same or different and are independently chosen from H or C1-C10 alkyl group; the kudzu-vine root daidzein-7, 4'-dioxo acetic acid compound, and a carrier or excipient which can be acceptable medically are combined to form medicine composite; the compound and the medicine composite has the advantages of cerebral ischemia resistance, oxygen-poor resistance, myocardial ischemia resistance, antagonistic dysmnesia resistance, platelet aggregation resistance and thrombopoiesis resistance and protecting rat cortical neuron damage caused by oxygen deficit.
WO2013191144A1 Novel indanesulfamide derivative A novel indanesulfamide compound, such as N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]- sulfamide, N-[(1S)-2,2,4,7-tetrafluoro-2,3-dihydro-1H- inden-1-yl]sulfamide and (+)-N-(2,2,4,6,7- pentafluoro-2,3-dihydro-1H-inden-1-yl)sulfamide, or a pharmaceutically acceptable salt thereof has an effect of improving the severity (score) of an attack in a mouse kindling model and therefore can be expected to serve as a therapeutic agent for epilepsy.
US20080009552 Markers of pre-term labor The invention relates to novel markers of pre-term labor, methods for assessing the status of pre-term labor using the markers, and methods for the diagnosis and therapy of pre-term labor.
WO2012175002A1 Derivate, preparation method and use of 10-methoxycamptothecine Provided is a 10-methoxycamptothecine derivate of formula (1), wherein R is selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, aryl substituted C1-6 alkyl, phosphate substituted C1-6 alkyl, amino-substituted C1-6 alkyl, carboxyl substituted C1-6 alkyl, hydroxyl substituted C1-6 alkyl, and amide-substituted C1-6 alkyl; R1 is selected from hydrogen and t-butoxycarbonyl substituted amino. Also provided in the present invention are the preparation method of the derivate and use thereof in anti-tumour drug preparation.
EP2364148A1 Combination of rocaglamide and apoptosis inducing substances for the treatment of cancer The present invention relates to a combined preparation comprising at least one rocaglamide derivative and at least one apoptosis inducing agent, preferably from the group of substances comprising agents inducing the extrinsic apoptotic pathway, antiproliferative agents and agents which induce apoptosis in T-cells by activation induced cell death (AICD) for the treatment of cancer.
US7741372 Targeting p38 mitogen activated protein kinase (MAPK) cellular signaling pathway; using such as N,N'-bis(3,5-diacetylphenyl)decanediamide tetrakis(amidinohydrazone) tetrahydrochloride There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target for intervention. There is further disclosed a use for guanylhydrazone-substituted compounds to treat diseases and disorders related to T cell activation and HIV-infection.
CN1915222A Composition of liposome, and preparation method A liposome composition used to prepare the medicines for treating tumor, cardiovascular and cerebrovascular disease, altitude ischemia and insomnia is prepared from the mixture of aspirin, prostaglandin E1, antioxidant, 2-hydroxypropyl-beta-dextrin and gamma-dextrin, the mixture of hydrogenated soybean lecithin and yolk lecithin, and the mixture of soybean sterol, polyethanediol-2000, VC and glycine. Its preparing process is also disclosed.
US8076361 Form of S-omeprazole The present invention relates to a novel form of the (−)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2 -pyridinyl)-methyl]sulfinyl]-1H-benzimidazole, i.e. S-omeprazole. More specifically, it relates to a novel form of the magnesium salt of the S-enantiomer of omeprazole trihydrate. The present invention also relates to processes for preparing such a form of the magnesium salt of S-omeprazole and pharmaceutical compositions containing it. Furthermore, the present invention also relates to new intermediates used in the process.
CN1723898A Fibranine gel, and its prepn. method An antisepsis and inflammation-relieving huangtensu gel for treating the gynopathic inflammation is prepared proportionally from huandensu, thickening agent, antiseptic, pH regulator, stabilizer, diluents and humcant.
CA2168203C Medicinal for protection from neurological damage This invention relates to a method of protection from and treatment of neurological damage in mammals by administration of dimethylsulfoxide (DMSO) in combination with fructose 1,6-diphosphate (FDP).
WO2007082806A1 Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine useful for the treatment of alzheimer’s disease via gaba receptors The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula (I): wherein R1 is hydrogen, halogen, hydroxy, lower alkyl, benzyloxy or -O-(CH2)-(CO)-5 or 6 membered heteroaryl optionally substituted by aryl or by lower alkyl; R2 is hydrogen, halogen, lower alkyl, lower alkynyl, amino, -NHC(O)-Ra or -(CO)-Ra; R3 is hydrogen, halogen, cyano, lower alkyl, lower alkynyl, amino, -NHC(O)-Ra, -(CO)-Ra, -5 or 6-membered heterocycloalkyl in 1-position, optionally substituted 10 by =O or is a -5 or 6-membered heteroaryl in 1-position; R4 is hydrogen or -5 or 6-membered heteroaryl; R5 is lower alkyl or cycloalkyl; Ra is lower alkoxy or NR'R'', wherein R' and R'' are each independently hydrogen, lower alkyl optionally substituted by hydroxy, lower alkynyl, -(CH2)n-cycloalkyl, 15 -(CH2)n-5 or 6-membered heterocycloalkyl or -(CH2)n-5 or 6-membered heteroaryl; n is 0 to 3; as well as pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
CN102038668A Lauric acid diethanolamide and application of analog thereof The invention belongs to the technical field of medicines, and relates to lauric acid diethanolamide and application of analog thereof, in particular to lauric acid diethanolamide, antibacterial activity of analog thereof, and application to strengthening of antibacterial activity of an antibacterial agent. The lauric acid diethanolamide and the analog thereof have structural general formulae shown as graphs (I and II) in the specifications, wherein the R group in the graph II is a straight-chain and branched alkyl groups with the 2 to 6 carbon atoms. The compounds have stable structures, and the compounds and the proper medical auxiliary materials are mixed so as to prepare various clinically acceptable preparations. Antibacterial experiment results prove that: the compounds have strong antibacterial activity, the effect of strengthening the antibacterial activity of the antibacterial agent to certain extent, and the advantages of strong activity, small dosage and the like. The lauric acid diethanolamide and the analog thereof can be used for preparation of antimicrobial medicaments and application of synergist of the antibacterial agent to preparation of the antimicrobial medicaments.
CN102600158A Medicine composite The invention relates to a medicine composite consisting of sibelium or cinnarizine and pyrrolidone brain metabolism improved medicine which are active ingredients, and pharmaceutically acceptable auxiliary materials, and application of the composite in terms of preparation of medicines for treating post-traumatic brain syndrome, sequelae of cerebral hemorrhage and cerebral infarction, cerebral arteriosclerosis, craniocerebral postoperative brain dysfunction, cerebrovascular accidental consciousness disturbance, hypomnesia, senile dementia and the like.
US20120282180 Compounds with Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.
CA2259353C Plaster for the transdermal application of pergolide The invention relates to a patch for transdermal application of pergolid and its pharmaceutically acceptable salts.
WO2009068668A1 New therapeutic approaches for treating cmt and related disorders The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related disorders. More particularly, the invention relates to combined therapies for treating said disease by affecting PMP22 expression in a subject.
CN102731344A Hydrazine nitrile cathepsin inhibitors with different P<3> structures, and application thereof The invention which belongs to the field of the design and the synthesis of cathepsin (Cat for short) inhibitors concretely relates to novel and efficient hydrazine nitrile inhibitors with different P<3> structures directed to four Cats (K, B, L and S). The main structure of the hydrazine nitrile inhibitors in the invention is represented by a formula in the specification; and in the formula, R1 is isobutyl, and R2 is alkyl, aryl, or cycloalkyl. The peptidomimetic hydrazine nitrile inhibitors designed and synthesized in the invention have the advantages of relatively simple structure, and easy synthesis; and the design and the synthesis of the maternal structure provide great conveniences for the synthesis of subsequent end products. Synthesized compounds, which can effectively inhibit actives of the Cat K, the Cat B, the Cat S and the Cat L, have an inhibition constant to the Cat K and the Cat L being in a picomole concentration (10<-12>M) level; and the synthesized compounds, which have weak inhibition effects on the Cat B and the Cat S have an inhibition constant being in a nanomole concentration (10<-9>M) level.
US20060004010 Ccr4 antagonist and medical use thereof A compound of formula (I) or a salt thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound of formula (I) has CCR4 antagonistic activity, and therefore is useful as a preventive and/or therapeutic agent for diseases associated with CCR4, i.e., CCR4-mediated diseases such as inflammatory and/or allergic diseases [e.g., systemic inflammatory response syndrome (SIRS), anaphylaxis or anaphylaxis-like reaction, allergic vasculitis, reject reaction for graft organ, hepatitis, nephritis, nephrosis, pancreatitis, rhinitis, arthritis, inflammatory ocular diseases, inflammatory bowel diseases, diseases in cerebro and/or circulatory system, respiratory diseases, dermatic diseases, autoimmune diseases, etc.], and the like.
US20100272709 Cathepsin l mediated diseases and associated methods and products This invention relates generally to the treatment of cathepsin or dynamin mediated diseases, such as proteinuria, cancer, and cognitive disease and related products. Diagnostic and other assays are also provided, as well as methods for podocyte cell gene transfer.
WO2012069658A3 Immunomodulatory compositions comprising hydralazine for the treatment gastrointestinal disorders Immunomodulator formulations for use in the treatment of disease of the Gl tract. The formulations comprise a hydroxylase inhibitor and/or an immunosuppressant. Exemplary formulations comprise hydralazine as a hydroxylase inhibitor and/or cyclosporin A as an immunosuppressant.
US20110196318 Gel-based phenergan composition and method of delivery The invention is directed to a system for treating vomiting comprising a topical gel placed within a syringe. The topical gel includes (a) between 10 to 40% Phenergen by weight, (b) between 30 to 50% of lecithin isopropyl palmitate solution by weight, and (c) between 30 to 70% of pluronic gel by weight. The syringe includes a cylindrical chamber having a front end, a back end, an interior side and exterior side. The syringe has a disposing opening located on the front end of the cylindrical chamber; a stopper of a sufficient size and dimension to engage the disposing opening; a plunger located within the cylindrical chamber; a rigid shaft having a sufficient size and dimension to fit within the cylindrical chamber and a plate affixed to a distal end of the rigid shaft. The syringe is plastic having a dark color to prevent degradation of the topical gel.
US7138533 acetylcholinesterase inhibitory action and an alpha 1 antagonistic action Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
WO2007136668A9 N-benzoyl-and n-benzylpyrrolidin-3-ylamines as histamine-3 antagonists The present invention provides a compound of Formula (I) and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
US7172756 Methods of promoting tolerogenic immune responses and compositions therefor Methods and compositions for promoting tolerogenic immune responses or treating immune responses to food antigens comprise Lactobacillus GG. Oral administration of Lactobacillus GG to patients such as human infants may promote a tolerogenic immune response to antigens in cow's milk.
DE102007061797A1 Method for gestagen treatment of hyperplastic process in endometrium, comprises selecting individual case-specific preparation, producing cytosolic fraction, detecting progesterone receptor level and measuring extent of specific binding Method for gestagen treatment of hyperplastic process in an endometrium, comprises: selecting an individual case-specific preparation on the basis of an individual assessment of the binding properties of progesterone receptor in the endometrium; producing a cytosolic fraction from the tissue of the endometrium of a specific patient; detecting the level of progesterone receptor in the cytosolic fraction, according to a radioligand method; and measuring the extent of the specific binding of the preparation with the produced progesterone receptor. Method for gestagen treatment of hyperplastic process in an endometrium, comprises: selecting an individual case-specific preparation on the basis of an individual assessment of the binding properties of progesterone receptor in the endometrium; producing a cytosolic fraction from the tissue of the endometrium of a specific patient; detecting the level of progesterone receptor in the cytosolic fraction, according to a radioligand method; and measuring the extent of the specific binding of the preparation with the produced progesterone receptor, where a compound with a greater value of extent of the specific binding, is used as a selective preparation. An INDEPENDENT CLAIM is included for the preparation for the treatment of hyperplastic process in the endometrium. - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : Progesterone receptor binder.
CN1954806A Teprenone orally disintegrating tablet prescription and its preparation method An oral disintegrating tablet of teprenone contains teprenone, filler chosen from MCC, dextrin, lactose and mannitol, disintegrant chosen from L-HPC, PPVP, CMS-Na and their mixture, flavouring chosen from nature or artificial sweetening agent, antioxidant chosen from VC, VE and BHA, lubricant chosen from magnesium stearate, magnesium lauryl sulfate and talc powder, and flowing aid chosen from superfine silicon gel powder and talc powder. Its preparing process is also disclosed.
US20070253946 Axon Regeneration Promoter An axon regeneration promoter is disclosed that contains an inhibitor of RGM-like protein as an effective component. Inhibitors of RGM-like protein encompass inhibitors of RGM-like protein such as anti-RGM-like protein antibodies and Y27632, as well as antisense nucleic acids and double-stranded RNAs that can inhibit the transcription or translation of RGM-like protein. The axon regeneration promoter according to the present invention is effective for the regeneration of central nerve axons and thus contributes, for example, to the treatment of patients who have suffered damage to the central nervous system, for example, the spinal cord, due to, for example, a traffic accident or a cerebrovascular disorder.
EP1059930B1 Compositions comprising isovaleramide and ibuprofen Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and its pharmaceutically acceptable salts, esters, and substituted amides, and other valerian-related compounds, in combination with NSAIDs exhibit clinically significant pharmacological properties which implicate a treatment for acute muscular aches, strains, and sprains which occur from a localized, external insult to a particular muscle or muscle group outside of, or peripheral to, the CNS. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.
CN101362715B Preparation method of N-acetyl-5-methoxytryptamine The invention discloses a method for preparing N-Acetyl-5-Methoxyl Tryptamine, which comprises the steps that: 5-Methoxyl Tryptamine and acetic anhydride are used as raw materials and absolute ethanol is used as a solvent; the N-Acetyl-5-Methoxyl Tryptamine is obtained by ordinary acetylation. The preparation method uses the absolute ethanol for replacing dichloromethane as the solvent, thus being safe, nontoxic, and the like, and reducing the pollution or contamination to human bodies or surrounding environment to the utmost extent; therefore, the obtained product is safer and can effectively improve the sleeping quality of patients.
WO2008059197A3 Topical composition comprising an anti- inflammatory steroid and a non-steroidal anti -inflammatory drug Use of an anti-inflammatory steroid and a non-steroidal anti-inflammatory drug in the manufacture of a medicament for topical application to a joint of a patient. The medicament may be for treating pain and inflammation at said joint and may be for treating inflammatory arthritis, osteoarthritis or rheumatoid arthritis at said joint. The medicament may be in the form of a transdermal patch.
CN103446086A Application of Incarviatone A in gastric cancer treatment drug The invention discloses application of Incarviatone A in preparation of a gastric cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Incarviatone A also has remarkable inhabiting effect on growth of human gastric cancer cell strains HGC-27, MGC-803, BGC-823 and SGC-7901. Therefore, the Incarviatone A can be used for preparation of an anti-gastric cancer drug and has good development and application prospect. The application of the Incarviatone A in the preparation of the gastric cancer treatment drug is disclosed for the first time. Due to the fact that the fact that the skeleton type is a novel skeleton type, and the high gastric cancer cell inhibiting activity of the Incarviatone A is previously unimagined.
US20080038296 Targeted delivery of drugs, therapeutic nucleic acids and functional nucleic acids to mammalian cells via intact killed bacterial cells A composition comprising intact killed bacterial cells that contain a therapeutic nucleic acid, a drug or a functional nucleic acid is useful for targeted delivery to mammalian cells. The targeted delivery optionally employs bispecific ligands, comprising a first arm that carries specificity for a killed bacterial cell surface structure and a second arm that carries specificity for a mammalian cell surface receptor, to target killed bacterial cells to specific mammalian cells and to cause endocytosis of the killed bacterial cells by the mammalian cells. Alternatively, the delivery method exploits the natural ability of phagocytic mammalian cells to engulf killed bacterial cells without the use of bispecific ligands.
US20080027088 Imidazole-Based Hmg-Coa Reductase Inhibitors The present invention relates to methods of treating atherosclerosis, dyslipidemia, other cardiovascular diseases and related diseases, such as diabetes, using a serine palmitoyltransferase (SPT) inhibitor. The present invention also relates to pharmaceutical compositions and kits that comprise a serine palmitoyltransferase (SPT) inhibitor, optionally with another pharmaceutical agent.
CN102552135A Method for preparing vitamin K1 emulsion, and vitamin K1 emulsion The invention relates to a method for preparing a vitamin K1 emulsion, and a vitamin K1 emulsion. The emulsion provided by the invention comprises components of: 0.5-2% of vitamin K1, 7.5-15% of soybean oil, 0.8-2% of phosphatide, 1.5-3% of glycerin, and balance of water. The pH value of the emulsion is 3.5-7.0. The method provided by the invention comprises a step for regulating the pH value of the emulsion composition to 3.5-7.0. The vitamin K1 emulsion provided by the invention has good medicine properties.
CN101890025A Application of gestodene in preparing emergency contraceptive medicaments The invention relates to novel application of gestodene, in particular to application of the gestodene in preparing emergency contraceptive medicaments, and the medicaments prepared by using the application.
US20110224723 Cyanoacrylate tissue adhesives A tissue adhesive including cyanoacrylate and polyethylene glycol (PEG), wherein the PEG remains a polyether and wherein the tissue adhesive is bioabsorbable. A tissue adhesive including cyanoacrylate bulk monomer and cyanoacrylate nanoparticles containing a therapeutic therein. A kit for applying a tissue adhesive, including the tissue adhesive described above and an applicator. Methods of accelerating degradation of a cyanoacrylate tissue adhesive applying a tissue adhesive, closing an internal wound, administering a therapeutic to tissue, treating cancer, and preventing infection in a wound. Methods of method of making a bioabsorbable tissue adhesive and making a therapeutic tissue adhesive.
CN103520137A Compound teriflunomide transdermal patch for treating rheumatic arthritis, and preparation method thereof The invention discloses a compound teriflunomide transdermal patch for treating rheumatic arthritis, and a preparation method thereof, and belongs to the technical field of medicines. The compound teriflunomide transdermal patch for treating rheumatic arthritis is composed of a back lining layer, a medicine storage layer and an anti-adhesive layer, wherein the medicine storage layer is mainly prepared from the following raw material drugs in parts by weigh: 0.55-12 parts of teriflunomide, 0.55-12 parts of non-steroid anti-inflammatory drug, and 100 parts of pressure-sensitive adhesive. The compound teriflunomide transdermal patch can be used for avoiding irritation of an oral drug to gastrointestinal tracts, increasing the percutaneous permeability of the drug by an ion-pair technology, has a durable and stable curative effect, and can be used for treating rheumatic arthritis and pains caused by the same; if administration is interrupted, the patch can be peeled off, and the use is convenient; the patch is good in adhesion and flexibility.
EP1975162A1 Oxazolone derivative Novel raw material compounds are provided that are useful for producing novel cycloalkane carboxamide derivatives having cathepsin K inhibitory action. An oxazolone derivative represented by formula (I): [wherein, R1 represents a substituted or unsubstituted alkyl group, substituted or unsubstituted alkenyl group, substituted or unsubstituted alkynyl group, substituted phenyl group, substituted or unsubstituted naphthyl group or substituted or unsubstituted heterocyclic group, and ring A represents a saturated cyclic alkylidene group having 6 to 7 carbon atoms].
CN103342757A Amphipathic chondroitin sulfate derivative and preparation method and application thereof The invention discloses an amphipathic chondroitin sulfate derivative which is good in internal absorption effect, high in bioavailability and stable in curative effect, and a preparation method and application thereof. The average molecular weight (Mw) of the amphipathic chondroitin sulfate derivative is 3,100 to 50,000 Da; the general formula of the derivative is shown in the specification, wherein x refers to the number of carbon atoms and is an integer between 10 and 22; y refers to the number of double bonds and is an integer between 0 and 6; n is an integer between 8 and 150; and the degree of substitution of O-alkyl ranges from 5% to 50%.
WO2012025761A1 Theobromine in combination with an expectorant or a mucolytic for use in therapy An agent comprises theobromine and an expectorant, or an agent comprises theobromine and a mucolytic. The agents of the invention may be used as a combined preparation for simultaneous, sequential or separate use in the therapy of cough.
CN101590072B Application of calycosin-7-O-beta-D-glucopyranoside or salt thereof in resisting AIDS The invention belongs to the technical field of medicaments, and discloses novel medicinal application of calycosin-7-O-beta-D-glucopyranoside or salt thereof. Pharmacologic tests improve that the calycosin-7-O-beta-D-glucopyranoside or salt thereof has the effect of resisting AIDS virus, can treat AIDS, and can be applied in preparing medicaments for resisting the AIDS.
CN101906121A Bacteriostatic component extracted from ageratum conyzoides and extraction method thereof The invention discloses a bacteriostatic effective component isorhamcomin-3-O-glucoside of ageratum conyzoides and an extraction method thereof. The isorhamcomin-3-O-glucoside belongs to flavonoid glycoside compounds, has the bacteriostatic function and can be used as a contrast substance for measuring the content of the ageratum conyzoides. The invention lays the foundation for developing a novel product of an ageratum conyzoides preparation aiming at improving the quality control standard of the medicinal material of the ageratum conyzoides.
US20110288060 apparatus and process for producing crystals This invention provides an oscillating baffled reactor apparatus for preparing crystalline particles of at least one substance comprising: a reactor vessel; means for supplying a first flowing stream; means for oscillating fluid within the reactor vessel; a plurality of baffles; source of ultrasonic radiation; and means for collecting said particles.
EP2170335A1 Compositions comprising tryptophan hydroxylase inhibitors Methods and compositions comprising tryptophan hydroxylase inhibitors are disclosed. Particular methods are directed at reducing or avoiding serotonin-mediated adverse effects associated with some drugs.
WO2010127557A1 Use of lanostanes and extracts from poria cocos for treating cachexia A pharmaceutical composition for treating cachexia, especially cachexia induced by cancer, comprising lanostanes as effective constituents. The suitable source of the lanostanes is the extracts from Poria cocos which comprise 1-60% (by weight) lanostanes without secolanostanes substantially. The extracts are extracted from the metabolite, fermented product or mycelium of Poria cocos (Schw) Wolf (Polyporaceae plant).
US20120004187 Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament The invention relates to spirocyclically substituted 1,3-propane dioxide derivatives, and to the physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, A and X are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
US20050261259 Phytosterol and/or phytostanol derivatives The present invention relates to a phytosterol and/or a phytostanol ester compound produced from the reaction of a phytosterol and/or a phytostanol with a polyunsaturated fatty acid (PUFA), wherein the polyunsaturated fatty acid has from 18 to 22 carbon atoms and at least three carbon-carbon double bonds. Processes for producing and compositions and a process for using such compositions are also provided.
WO2006063801A1 Novel polymorph of (5-amino-6-methoxy-3-pyridincarbonyl)carbamic acid 2-(s)-hydroxymutilin 14-ester The present invention relates to a novel polymorph, to processes for the preparation of the polymorph and to the use of the polymorph in medicine, particularly antibacterial therapy.
WO2006082053A1 7-ethyl-10-hydroxy-camptothecin lipid ester derivatives The subject of the present invention are specific lipidesters of 7-ethyl-10-hydroxycamptothecin, their preparation, pharmaceutical compositions containing such compounds and the use of such lipidesters in the treatment of tumors.
US7365073 3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4 Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
US20130041016 Compositions and Methods for Preventing and Treating Cancer via Modulating UBE1L, ISG215 and/or UBP43 Compositions and methods of using compositions that induce UBE1L or a ubiquitin-like protein ISG15, or inhibit a deconjugase UBP43 to degrade oncogenic proteins and enhance apoptosis of cancer (neoplastic) or pre-cancerous (pre-neoplastic) cells are provided. Methods for the prevention or treatment of cancer via administration of these compositions are also provided.
EP1539176A1 Thiazine and oxazine derivatives as mmp-13 inhibitors for treating arthritis A compound selected from those of formula (I): wherein: • X1, X2, and X3 represent nitrogen or -CR3 in which R3 represents hydrogen, alkyl, amino, alkylamino, dialkylamino, hydroxy, alkoxy, or halogen, • Gl represents oxygen or S(O)p in which p is from 0 to 2, • G2 represents carbon-carbon triple bond, C=O, C=S, S(O)q in which q is from 0 to 2, or a group of formula (i/a): in which YI and Y2 are as defined in the description, • n is fromO to 6, Zl represents -CR4R5, wherein R4 and R5 are as defined in the description, • A represents 5- or 6-membered monocycle or bicycle aryl, heteroaryl, cycloalkyl, or heterocycloalkyl, • RI represents hydrogen, alkyl, alkenyl, alkynyl, (these groups may be optionally substituted as defined in the description) or the group of formula (i/b): in which s, Z2, B, t and G3 are as defined in the description, and optionally, its optical isomers , N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease, for the treatment of i.a arthritis and cancer.
CN102114082A Compound giant knotweed emulsion for preventing livestock and poultry infection The invention relates to a compound giant knotweed emulsion and a preparation method thereof. The emulsion of the invention can be administrated by drinking, and stock solution after being diluted can be evenly dispersed in water and can be kept in a stable state. The emulsion is used for treating escherichia coli mixed infection, and simultaneously for effectively restoring internal damaged mucous membrane. The invention has the effects of fast sterilization, pain relieving, haemostasis and the like, obvious exterior syndrome relieving. In addition, the compound giant knotweed emulsion used with astragalus mongholicus polysaccharide also has the advantages of virus resistance, strengthening resistance, fast effectiveness, good curative effect, little drug resistance of the livestock , no recurrence after curing and the like.
US20080214602 N-Biarylamides The invention relates to N-biarylamides useful for the prophylaxis and/or treatment of impairments of perception, concentration, learning and/or memory, and to processes for preparing them, and pharmaceutical compositions containing them.
CN101724038A Human epididymis expression sperm binding protein HEL-5, encoding gene and application thereof The invention belongs to the field of biotechnology and medicine, and discloses a new human epididymis specific expression sperm binding protein HEL-5 as well as preparation and application thereof. The invention discloses an amino acid sequence of the HEL-5 protein and provides a recombination expression vector carrying the DNA sequence for encoding the protein. The invention also discloses a preparation method of the protein and a method for detecting the biological function of the HEL-5 protein. The protein has low-abundance expressed in the epididymis, is combined on the surface of sperm and has important function for protecting the sperm, normal fertilization and early embryonic development. The HEL-5 protein can be used as a target protein for researching and developing immunity contraceptive as well as clinical diagnosis and treatment for male sterility. A method for detecting a corresponding gene or protein based on development of the HEL-5 protein can be widely used for the research field of reproductive medicine.
CN102245166A Ophthalmic administration of a composition including brimonidine as a mist Disclosed are methods of treatment including administration of a pharmaceutical composition including brimonidine to an eye as a mist, the composition devoid of a penetration enhancer.
US20070197602 Combined pharmaceutical composition At least one hyperlipidemic agent selected from the group consisting of a fibrate compound (e.g., fenofibrate, bezafibrate, or a salt thereof) and an HMG-CoA reductase inhibitor (e.g., a statin compound, for example, pravastatin, atorvastatin, or salts thereof) is, as active ingredients, combined with an α-glucosidase inhibitor (e.g., voglibose, and acarbose) in the pharmaceutical composition of the present invention. The proportion of the α-glucosidase inhibitor may be about 0.001 to 50 parts by weight relative to 100 parts by weight of the hyperlipidemic agent. The present invention provides a pharmaceutical composition which is excellent in prophylactic and/or therapeutic effect on metabolic syndrome, hyperlipemia, diabetes, diabetes complications, etc, and has few side effects.
US20100234289 Integrin binding rgd-lipopeptides with gene transfer activities The present invention provides synthesis of a novel series of cationic lipopeptides with integrin-binding RGD functionalities. The invention also provides high L27 (transformed S1 80, mouse sarcoma cells) cell tropic gene transfer properties of these novel RGD-lipopeptides. Since 127 cell surface contains over expressed integrins, the present class of lipopeptides with integrin-binding RGD ligands are likely to find future applications in targeting anti-cancer genes/drugs to the endothelial cells of tumor vasculatures (possessing over expressed integrins).
CN1927345A Antifungal liquid drug The invention discloses antifungal liquid for treating various fungus skin diseases, wherein each 500ml of the soup includes euphorbic acid 0.5-0.7g, radix salvia miltiorrhiza 0.3-0.4g, chrysanthemum flower 0.5-0.8g, cinnabar 0.2-0.4g, borneol 0.3-0.4g, Chinese dittany bark 2-2.5g, clove 0.5-0.8g, Chinese gall 0.5-0.6g, orpiment 0.2-0.3g and bulb of edible tulip 1g.
WO2006124813A3 Substituted 7, 8-dihydro-1h-pyrimido [4,5-b] [1,4] diazepin-4-amines as?kinase inhibitors Compounds having the Formula (I) are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
EP1659116A1 Fki-1366 substances and process for producing the same A microorganism belonging to Beauveria sp. and having ability to produce FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C (Beauveria sp. FKI-1366 FERM BP-08459) is cultured in a medium, accumulating FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C in the culture liquid and isolating FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C from said cultured mass. Since the thus obtained FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C or composition thereof have activity to enhance azole antifungal agent, the substance has an action against various fungal infections such as deep-seated mycosis and other fungal infections in the low concentration within short term. Consequently, the substance is useful for reducing frequency of appearance of resistant microorganisms and overcoming resistance, and is expected as a medicament.
US20090326069 Azelaic acid ester compositions and methods for diagnosing and treating tissue conditions using azelaic acid ester compositions and proteinaceous biomarkers Therapeutic and cosmetic treatments are performed through the application of azelaic acid ester compositions to patients suffering from or exhibiting tissue inflammation. The diagnosis, characterization and treatment of a patient suffering from or exhibiting tissue inflammation may be enhanced by using selected proteinaceous biomarkers obtained from analysis of said markers by means of multiplexed immunoassay and comparison to the biomarker levels of healthy tissue.
US20100273729 Compositions Comprising Compounds Of Natural Origin For Damaged Skin The present invention relates to a skin-protecting composition for the damaged skin, comprising glycyrrhizin, quercetin, rosmarinic acid, madecassic acid, chamazulene, bicalein and emodin. The composition of the present invention has all of excellent antioxidant, anti-inflammatory, wound-healing and moisturizing effects, thereby being widely used in medicine, cosmetic material or the like for the purpose of protecting the easily infectable, damaged and dried skin.
CN101804052B Liposome injection based on drug combination of mezlocillin sodium and sulbactam sodium The invention provides a liposome injection based on a drug combination of mezlocillin sodium and sulbactam sodium. The liposome injection comprises the following components: mezlocillin sodium, sulbactam sodium, liposome carriers, frozen and dried supporting agent and optional existing antioxidant, wherein the liposome carriers are particularly hydrogenated soybean phosphatidylcholine and octadecylamine. The liposome injection of the invention has good preparation stability, prevents the liposome from being cracked under the action of dehydration, fusion and ice crystal generation in the freezing-drying process, and keeps good entrapment rate of the liposome after re-dissolution through hydration.
CA2412885C Porous celecoxib matrices and methods of manufacture thereof Celecoxib is provided in a porous matrix form wherein the dissolution rate of the drug is enhanced when the matrix is contacted with an aqueous medium. The porous matrix yields upon contact with an aqueous medium nanoparticles and microparticles of celecoxib having a mean diameter between about 0.01 and 5 µm and a total surface area greater than about 0.5 m2/mL. The dry porous matrix preferably is in a dry powder form having a TAP density less than or equal to 1.0 g/mL. The porous celecoxib matrices preferably are made using a process that includes: (i) dissolving celecoxib in a volatile solvent to form a drug solution; (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution; and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the dry porous matrix of celecoxib. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug.
CN102698223A Vinegar-ginger paste for removing beriberi The invention discloses vinegar-ginger paste for removing beriberi. The vinegar-ginger paste for removing the beriberi comprises the following components: 2.4 to 2.5 kg of vaseline, 1.8 to 1.9 kg of vinegar essence, 2.2 to 2.3 kg of old ginger and 4.2 to 4.3 kg of bran powder. The vinegar-ginger paste for removing the beriberi is easy to make and low in cost, and has no toxicity or harm to human bodies and has a good beriberi removing effect.
US20100143456 Model membrane systems The present invention relates generally to modifying biological and/or synthetic membranes or liposomes, or combinations thereof, for the purpose of altering immunity, or for the targeting of drugs and other agents to a specific cell type or tissue when administered in vivo to achieve a therapeutic effect. Modification of the membranes is achieved by incorporation and/or attachment of metal chelating groups, thereby allowing engraftment of one or more targeting molecules possessing a metal affinity tag, and a targeting of the engrafted membranes to specific cell types or tissues in vivo. The invention, thus, provides a means of modifying the properties of biological and/or synthetic membranes and liposomes for the purpose of altering or enhancing immunity when used as vaccines, or for the targeting of encapsulated/incorporated drugs or other agents to a specific cell type or tissue when administered in vivo, to achieve a therapeutic effect or response, or for modifying a physiological response or biological function.
WO2009116086A3 Topical formulation comprising adapalene microspheres and clindamycin The present invention relates to stable fixed dose topical formulations comprising an antiacne agent and an antibiotic, which exhibit storage stability at a temperature of about 40 °C and relative humidity of about 75 % for a period of at least 3 months. Particularly, the present invention relates to stable fixed dose topical formulations comprising therapeutically effective amounts of (a) adapalene-containing microspheres and (b) clindamycin, a process for their preparation thereof and their use for the treatment of acne.
WO2012014524A1 Sugar metabolism improving composition, and pharmaceutical preparation containing said composition The purpose of the present invention is to provide a highly safe composition that improves glucose tolerance and sugar metabolism at skeletal muscles, and a prevention/treatment drug for diabetes/metabolic syndrome containing the composition. Provided is a composition that is for improving sugar metabolism and glucose tolerance and that contains a compound represented by formula (I) derived from a plant selected from the group consisting of Rumex japonicus, R. crispus, and R. obtusifolius as the active ingredient.
US20090042993 Identification of novel post-translational protein modifications Compositions and methods for post-translational modifications that include protein acetylation in the ER lumen and deacetylation in the Golgi apparatus are provided. The disclosed methods are especially suited for the identification of compounds useful for the prevention or treatment of neurodegenerative diseases such as Alzheimer's.
CN102949559A Tincture for treating verruca plana The invention provides a tincture for treating verruca plana. The tincture is prepared by the following raw drugs in parts by weight: 25-35 parts of isatis root, 25-35 parts of rhizoma cyperi, 15-20 parts of safflower, 15-20 parts of mirabilite, 8000-1000 parts of alcohol with the mass fraction being 75%. A preparation method comprises the following steps of: adding 75% alcohol into the raw materials, sealing, soaking for 7 days, filtering, taking liquid medicine, and subpackaging with 20ml for each bottle. The tincture provided by the invention has the advantages of short treatment course, less side effect, simple operation, low price and good curative effect and the like, and is easily accepted by patients.
US20110003832 NEW CAPPED Pyrazinoylguanidine SODIUM CHANNEL BLOCKERS The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.
US20110126303 Modified Blood Clotting Factors And Methods Of Use The invention provides compositions including modified blood clotting factors that have a non-native proteolytic cleavage site engineered into them allowing intracellular cleavage and secretion of an active form. The compositions are useful in the methods for treating a bleeding or clotting disorder.
US20090175933 Preparation for the treatment of diarrhoea A preparation for the treatment of diarrhoea comprising a bulking agent and an anti-diarrhoeal agent wherein the anti-diarrhoeal agent is provided in the form of an anti-motility agent.
CN103735569A Medicament composition for treating scorpion black rot The invention provides a medicament composition for treating scorpion black rot, relating to the technical field of culture of special species. The medicament composition comprises the following components in parts by weight: 4-6 parts of baking soda piece, 0.8-1.2 parts of sulfanilamide and 1000 parts of mixed feed. The medicament composition for treating scorpion black rot, provided by the invention, is reasonable in compatibility, remarkable in treatment effect of the scorpion black rot, simple and convenient for medication, and low in treatment cost.
EP2044027A2 Fused bicyclic compounds interacting with the histamine h4 receptor Compounds that interact with the histamine H4 receptor, and which may be useful for treating or preventing disorders and conditions mediated by the histamine H4 receptor, e.g. inflammation, are of formula (I) wherein Q is CR1 or N; X is CR2 or N, provided that Q and X are not both N; Y is CR3 or N; Z is CH or N; R1, R2, R3, R4, R5 and R6 are independently H, F, Cl, Br, I, or a hydrocarbon group which optionally contains one or more heteroatoms; and R7 is a heterocyclic radical including one or more N atoms; or a pharmaceutically acceptable salt, ester or solvate thereof.
US20120252819 Solid dispersion formulations and methods of use thereof The present invention relates to formulations and methods for increasing the bioavailability of 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one, 1-(3,3-diphenylpropanoyl)piperazine, or a salt thereof. In particular, the formulation can include one or more pharmaceutically acceptable matrix polymers to form a solid dispersion, e.g., a spray dried dispersion or a hot melt extrusion.
US8765668 Methods of synthesis of β-aminobutyryl substituted compounds The present invention relates to process to prepare β-aminobutyryl compounds having β-amino acid core structural moieties and optionally having γ-phenyl and/or heterocyclic structural moieties. Such compounds are useful as key structure framework of modern drug chemistry.
CN1966042A Externally applied ointment for treating hyperosteogeny and preparation method thereof The invention relates to an external application pharmaceutical composition for treating osteoproliferation which comprises semen strychni, Sichuan aconite root, Kusnezoff monkshood root, jack-in-the-pulpit tuber, pinellia tuber, white pepper, buthus martensi karsch, Cinnamomum cassia, white mustard seed, datura flower, wood louse, dragon's blood resin, frankincense, myrrh, notoginseng, asaryl, black-tail snake, cassia twig, mulberry twigs, Chinese ephedra, large-leaf gentian root, peach kernels, safflower, ledebouriella root, spatholobus stem, Chinese angelica root, notopterygium root, pubescent angelica root, campeachy wood, earthworm, Clematis chinensis, curcuma longa, achyranthes root, pawpaw, Ligusticum wallichii, speranskia herb, burred tuber, Japanese yam, zedoary, pyrola, garden balsam seed and hairy birthwort.
CN101991586A Compound difloxacin hydrochloride injection as well as preparation method and application thereof The invention discloses a compound difloxacin hydrochloride injection as well as a preparation method and an application thereof. The compound difloxacin hydrochloride injection comprises the following components in parts by weigh: 5-20 parts of difloxacin hydrochloride, 0.25-5 parts of furosemide, 50-300 parts of ethanol, 50-300 parts of propylene glycol and 400-900 parts of water for injection; the preparation method comprises the following steps: successively dissolving the components; using hydrochloric acid or sodium hydroxide to adjust pH to 9.5-10.5; adding the water for injection to reach1000 parts to obtain the injection. The preparation prepared by the invention is stable, has wide antimicrobial spectrum, has quick and remarkable curative effect, and high bioavailability; and the experiment proves that the curative effect can be enhanced by the combining utilization of the difloxacin hydrochloride and furosemide; and the injection has wide clinical application, can be used as top choice for piglet hydropsy, and the livability of the piglet is improved and the morbidity is lowered.
CN101229299B Medicine promoting bone-knitting The invention discloses a medicine for promoting bone coaptation; the invention overcomes the defect of medicines in the prior art and utilize a new formula of multiple medical materials to prepare a pill for specially and effectively promoting bone coaptation. The components of the medicine are generally used medical materials in pharmacopoeia. The indigents of the invention and the corresponding weight of each indigent are as follows: sambucus williamsii hance of 20 to 30g, blood resin of 5 to 10g, himalayan teasel root of 10 to 15g, pyrite of 3 to 5g, RhizomaChuanxiong of 3 to 5g and panaxnotoginseng of 3 to 5g. The medicine preparation process is as follows: selecting and preparing raw medical materials, grinding the materials into fine power, using bee honey to stir the power to make into pills the same size as mung beans, and last filling the pills into jars. The preparation process is simple and available, practical and effective.
CN1817347A Medicinal composition with miglinon and proactidil as active components, and preparing method and use thereof A medicinal composition in the form of tablet, capsule, dispersing tablet, chewing tablet, disintegrating tablet, etc for treating diabetes B is prepared from pioglitazone hydrochloride, miglinar and the pharmacologically acceptable additives.
US20120108623 Beloxepin and analogs for the treatment of pain This present disclosure provides methods of treating pain with beloxepin and/or beloxepin analogs.
CA2633585A1 Treatments for any and all mental/brain neuron/spinal cord illness Treatments for Any and all Mental Illness We could try Ritalin, GABA and St. John's Wort, GSM (gamma-secretase modulators), Magnolia Bark (for infections and scarring as well) - as well for methane from livestock. Parkinson's We are looking (placing in the brain) at 1. warmer (to even out and/or flash to use intensity to pacify and smooth out calming; pacing and leading a steady buzz the nerves and chatter between misfiring neurons) micro chip electrode, and/or 2. acoustic to the skull (for vibrations) and/or 3. we can use DTI to and Neural Links to trace the patterns of the brain's activation process as each differing misfires are triggered, and thus anticipate the triggers and their expected spreading activation area of the brain and in addition 4. we can use electrodes (electro shock increase intensity and frequency - possibly for drug addicts and obesity, and OCD) and short circuit by pre-empting shakes/tremors (aimed at) caused by misfiring areas of the brains' neurons and literally drown out of the misfiring electrical charges thus allowing new neurons to build bridges that are not supported/dependent (based) on interactions/co-dependence - mind responses interconnected with the misfiring nerves. By shocking the brain areas of misfiring we hope to shake of the ingrained process (grooves) of misfirings neurons and also to allow healthy neurons to play a more dominant role as the brain starts to depend on the healthy neurons to strengthen the regulation of brain signals to body movements (the continuously largely random (background shakes) - except sometimes when trying to concentrate on moving eg. a hand which can trigger a tremor episode also trying to hold the hand steady and trying to suppress a segment of motion -perhaps trying to conduct a steady movement can perhaps trigger the tremors). 5. We can use stem cells (culture) with converted neuron cells, the stem cells can produce neutrophins that are all injected into the brain tissue/glands that are responsible for movements. 6. electro-magnetic waves... We could continuously modulate the levels of any of the above treatments so that the mind does not get used to the treatment and desensitizes. Alzheimer's To cure Alzheimer's we take a multi-pronged approach. 1. We electroshock the areas of the brain that have plaque (the electro-shock strong/powerful/and continuous (yet safe for most brain tissue - perhaps sacrificing some healthy brain tissue that share the same area as the plaque; lasting long enough to dislodge/loosen/shakeoff/to break up the plaque from sticking/clinging, possibly by adjusting the frequency of Electrode(s) Helmet and or we could try radiation, and/or topical anti-scarring substance and/or derm-abrasion and/or ECT and/or (Prolonged) TENS. We also use cell culture stem cells and their product neutrophins to inject into the formerly plaque areas to repopulate with healthy cells. Studies show that active minds playing puzzle games can keep the brain healthier. As thoughts escalate towards (recognition - which is based passed understanding) recognition of missing pieces from the patient's memory, a memory the requires the plaque area of the brain to register, we treat by initially with electro-shock the plaque areas, then wean to a calmer electro pulse (gentle less short circuit) - a stimulus escalating recall that mimics other healthy brains (measured/observed via DTI and neural links) escalate and go through the process of spreading activation, where the healthy brain would not be blocked at the place where the spreading activation should would use the same plaque part of the brain to recall to activate and recall that part of the brain where memory of a patient is blocked due plaque and/or other miswiring related to plaque in the Alzheimer's brain. To stimulate the brain to grow and prime new linkages around the missing and damaged memory recallability, we can bridge and train the to go from the escalation up to the block and then to feel the escalating (tip of tongue phenomena for the missing pieces), in synchronization with pulsing electro stimulus, and or heat flash (zing) high heat. The idea is to bypass the brain wiring that would be accessed and used recall memories that can't be recalled and grow new linkages (possibly using Neural Links/Artificial Intelligence/Computer/ -pacing and leading, reward and denial of impulse/satisfaction) that bypass and rather use healthy parts of the brain tissue (we could also use steady heat micro chip to other parts of the brain or neural links to either other healthy parts of the brain and/or the newly plaque cleansed and stem cells (neutrophins) renovated parts of the brain. Active Mind/Puzzles/Studying new Information to Keep Mind Healthy Longer Neural Links that Pace & Lead starting with puzzles where blocked (Artificial Intelligence or teacher supplies changing Memory Models - and/or website and/or algorithm adapting), (to test the patient's recognition's skill - therefore giving the patient practice in learning and recall short term and long term. Mental exercises such as Senduko and other puzzles, as over the courses of studying/learning and then testing, the Artificial Intelligence concludes the what and kind of information that is usually blocked (patterns in type of information, eg. math, when learning is hard - eg. many people can't study in public, complex concepts with many entities and interactions...), the Artificial Intelligence then suggests leads (eg. memory model clues) to the missing piece answers. When the remembered cues used to access a missing piece memory is correct the heat microchip warms up to create a pleasant feeling synchronized together in intensity - synchronized to recognition (gains -eureka) when you remember a missing piece so surely that you know the a part segment/group of a possibly larger memory that the patient is trying to remember. If the clues all lead to a dead end, then the Artificial Intelligence supplies (partially suggest/reveal based on what people usually use to identify) an entity and/or interaction. And as the patients' gets better the leads are revealed little by little in random. If the technology is used during free time (asleep ?) or even all day long and the mind looses focus (awareness loses track and hits memory block) - the stimulus reward for the brains' recognition includes heat and electro pulse to overcome inertial mental fatigue, where the patient's mind is under momentum in one direction/topic of recurring thought (OCD Obsessive Compulsive Disorder) or accessing in real and/or unnatural depression, both irritated easily and/or unable get the laziness out his/her mind where the state (An GV) is revisited in by appropriate (GV GP) frequency and/or duration, and/or forgets pieces that were already solved, the Artificial Intelligence reminds gently draws back focus (learning during downtime) the Artificial Intelligence/Neural Links can reward/deny reward via most probably vibrations (but also electro pulse and heat flash to reward), to wake up concentration if the person's attention starts to drift - needed to accept and retain information, the person's mind is navigated (programmed by healthy memory models), and then tested to answer questions/and operations, about the topic that their seem to have a strong grasp and rhythm relationship between parts that make up the system the particular missing part/answer belongs to without very many substitutes to and when the learning was under optimal conditions (eg. not worried about pass and/or fail, but motivated by reward (also curiosity) to understand the information and recall). When clues/attributes/linkages/connections are based on ranked by interest the patient is more motivated to try hard (and even harder and not give up) and even feel like they're are not even trying that hard because the material being learned and the enjoyment of the game/model/presentation of the material is fulfilling. Alzheimer's patients' seem to have trouble with recall of new information. One method is constantly review and at the same time use the treatments above to stimulate the brain to in synchronicity to mimic spreading activation of healthy brains. The length of time between review cycles depends on how quickly patient loses the memory. In normal people studying includes recognizing entities and/or interaction/operations, especially the memorable ones (GP GV)(landmarks/anchors), and how they relate to the missing part. The patient is tested, and reviews the missing parts (the parts that he has forgotten), then retests until all the information (especially with a focus on the forgotten/missing parts/pieces are remembered). Then the patient takes a 20 minute of studying different sections or even doing something completely different) break (repeating the study, review, break (consequitively longer breaks) and retest (refocus on the forgotten parts especially the ones that are constantly forgotten - mental block) and switch/alternate to full review to get all the information to cling to you're awareness, then retests restudying and creating new memory models to more multi-primed avenues of recall via unique clues that are easily grasped based usually on mastery of the attribute/clues/connections/linkages/leads (ranked by single uniqueness and ease to grasp and increase in strength caused by combinations of recognizable clues/leads). Heat flash and/or electro pulse reward when the patient remembers a belief that suggests lead - - perhaps by sticking to relevant leads and reviewing the memory model may not be as fast in patient's recall (stumbling onto memory blocks), but it avoids deviation from dead end key words that lead to unnecessary areas out side the schooling course that the patient is trying to master, however, using any and all clues/leads can create a grand scheme understanding of relationships and where and how...the information being studied fits into the what the patient knows about the world. The patient could participate in down time memory games and modulate key words and well as entities and interactions (glare/contrast). The aim is to stimulate the brain to create new ways of accessing/activating/growing/neurons firing in the brain that replace and/or create new path ways/spreading activations to allow the missing parts (often recent memory), to be encoded/programmed retained ultimately to the point the patient no longer needs aid. During the times of learning electro pulse, heat flash rises and falls at points of recognition of parts to segments towards enough estimated understanding wanted - mastery needed, and also looking back at memory search uses the same recognition process. The external stimulus provides a feeling of happiness, satisfaction at completing parts towards entire puzzle. The learning can be communicated via narrating, reading and or illustrated objects/entities/interactions (including moving), when the patient loses focus the key words...are revisited (to the place in learning and speed of recognition that usually signifies mastery except sometimes one or two key words/objects which are emphasized by higher volume, slower and over pronunciations spitting and vibrating and lengthening the gaps between pronunciations (phonetics), and when the mind wanders the Neural Links and Artificial Intelligence together with the stimulations emphasize what are key words/pictures/objects... that are being studied and provide the background (building blocks that the meaning/beliefs reveal in their basic place in the topic and/or subtopic being studies - the necessary understanding of objects/entities/interactions/operations information that a student should know before studying more complicated usages of the objects/entities/interactions/operations) ... of which which key pieces sinking in/being absorbed, loss of attention where the key words don't seem relate or address the questions that these words/pictures/objects should answer for the person's (relevant) purpose(s) and/or fall under the topic/sub-topic/section that they are found in...their relationship to that segment are unexplained. And/or the moment the mind wanders the significance of the words/pictures/objects' relationship and explanation of how it works are missed/bypassed/skipped during the duration of the mind's loss of comprehensionless loss focus.
US7358045 Using engrailed-2 (En-2) gene expression as a diagnostic and prognostic indicator of mammary gland cell proliferative disorders; antisense agents The present invention relates to a method for determining a predisposition to develop cancer in a patient, comprising the step of detecting EN 2 gene or its expression product in said patient or in a biological sample of said patient, whereby detecting presence of at least one of EN 2 gene or its expression product is indicative of a predisposition to develop breast cancer. The present invention also relates to antisense hybridizine to EN2 gene kits for determining predisposition to develop cancer and method of reducing EN2 expression.
WO2014011754A1 Novel 1, 4-benzoxazinone compounds The present invention provides novel benzoxazinone compounds, pharmaceutical compositions comprising such compounds, and methods of treating disease using such compositions. Pharmaceutical compositions of the invention are particularly useful in the treatment of neurodegenerative diseases.
US7897641 Propionyl L-carnitine and glycine, serine, alanine or arginine A composition is disclosed which is suitable for the prevention and/or treatment of cell and tissue abnormalities of exogenous, toxic or metabolic origin and suitable for reducing the toxic effects of cyclosporin-A and other immunosuppressive agents, which may take the form of a food supplement or of an actual medicine, containing as its active ingredients in combination or separately packaged: (a) propionyl L-carnitine or one of its pharmacologically acceptable salts, and (b) an amino acid selected from the group consisting of glycine, serine, alanine and arginine, or mixtures thereof.
CN101565446A Veratramine degradation product veratrum fluorene aldehyde and the derivatives thereof, as well as the preparation and application thereof The invention provides a veratramine degradation product veratrum fluorene aldehyde 1 and derivatives thereof. The invention uses steroidal alkaloid veratramine (A) as raw material and prepares veratrum fluorene aldehyde by oxidative degradation of m-chloroperoxybenzoic acid to obtain 20 derivative compounds of the veratrum fluorene aldehyde 1 after further oxidation, reduction and condensation reaction. The 20 compounds of the invention have good inhibitory activity on cancer cells, wherein the compounds 1, 2, 5, 8, 13 and 17 have good inhibitory activity on cells of human pancreatic cancer cells BxPC-3 and SW1990, small-cell lung cancer cells NCI-H446, human colorectal cancer LOVO and the like, and the inhibitory activity of the compound veratrum fluorene aldehyde 1 is the most significant.
WO2014147016A1 Ror gamma modulators The present invention relates to compounds of formula I, or a pharmaceutically acceptable salt thereof, characterized in that at least one of R8, R9, R10, R11 is -ORa; for use in the treatment or prevention, suppression or amelioration of a disease mediated by the ROR gamma receptor in a subject in need thereof, in particular diabetes and diabetes-related disorders, specifically type II diabetes, methods of their production, their use as a dietary supplement or functional food, as well as methods of treatment or prevention of such diseases.
CN102241675A (1R,3S)-1-(4-hydroxyl-3-methoxycarboxyl)-1,2,3,4-tetrahydro-beta-carboline-3-formyl amino acid derivatives as well as preparation method and application thereof In the invention, methyl 5-formyl-salicylate reacts with L-tryptophan benzyl ester, and then the obtained compounds is subjected to amino acid modification so as to obtain a series of (1R,3S)-1-(4-hydroxyl-3-methoxycarboxyl)-1,2,3,4-tetrahydro-beta-carboline-3-formyl amino acid derivatives and intermediates thereof; and the research on the anti-platelet aggregation activity and antithrombotic activity of the derivatives is performed. The method is simple, the used raw materials are available, safe and cheap; and the obtained product has anti-platelet aggregation activity and antithrombotic activity and is good for the development of anti-platelet medicaments. Therefore, the invention discloses the clinical application prospects of the (1R,3S)-1-(4-hydroxyl-3-methoxycarboxyl)-1,2,3,4-tetrahydro-beta-carboline-3-formyl amino acid used as an antithrombotic agent.
WO2006061378A1 Phenylpiperazine derivatives with a combination of partial dopamine-d2 receptor agonism and serotonin reuptake inhibition The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification, and tautomers, stereoisomers and N -oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N -oxides.
CN103126991A Voriconazole nano-micro composite powder and preparation method thereof The invention discloses voriconazole nano-micro composite powder, wherein a safe and reliable pharmaceutical auxiliary material is adopted to replace cyclodextrin, tween and other auxiliary materials generally-used in the current voriconazole preparations or physiologically toxic organic solvents as a solvent so as to improve product safety, the composite powder can be dispersed in water so as to obtain a transparent dispersion, and the drug has characteristics of high concentration, small particle size and easy absorption by human body. The present invention provides a voriconazole nano-micro composite powder preparation method, which has characteristics of simple operation, easy enlargement and industrial production, and good application prospect.
WO2009045655A3 Compositions containing purine nucleosides and manganese and their uses This invention encompasses methods of preserving protein function by contacting a protein with a composition comprising one or more purine nucleosides (such as e.g., adenosine or uridine) and an antioxidant (such as e.g., manganese). In addition, the invention encompasses methods of treating and/or preventing a side effect of radiation exposure and methods of preventing a side effect of radiotherapy comprising administration of a pharmaceutically effective amount of a composition comprising one or more purine nucleosides (such as e.g., adenosine or uridine) and an antioxidant (such as e.g., manganese) to a subject in need thereof. The compositions may comprise D. radiodurans extracts.
CN101429175B Perilla alcohol derivant with antineoplastic activity and uses thereof The invention discloses a perilla alcohol derivative with anti-tumor activity, which has a structure as right. The compound is obtained by using perilla alcohol as an initial raw material through chlorination reaction and condensation reaction. In vitro cell experiments show that the compound has propagation inhibiting effect on a cancer cell strain Lncap of human pancreas, is a potential anti-tumor medicament, and has application to preparing anti-tumor pharmaceutical preparations.
US20090247647 Method of Stimulating Proteoglycan Synthesis in Cells A method of stimulating the production of proteoglycans in a living animal cell comprising administering one or more Vitamin D3 metabolites to the living cells is provided.
CN103080080A 6,7-dihydro-5h-benzo[7]annulene derivatives, process for preparation thereof, pharmaceutical preparations comprising them, and the use thereof for production of medicaments The invention relates to selective estrogen receptor modulators (SERMs) and to processes for production thereof, to the use thereof for treatment and/or prophylaxis of disorders, and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, more particularly of bleeding disorders, osteoporosis, endometriosis, myomas, hormone-dependent tumors, for hormone replacement therapy and for contraception.
WO2012078210A1 Crth2 modulators and preparation thereof The present invention relates to processes and intermediates for the preparation of compounds useful as CRTH2 antagonists. Compounds prepared by the processes of the invention are of Formula (AI), (All) and Compound (I).
CN102206243A Medical application of ursolic acid-NF (Nuclear Factor)-kappaB inhibitor The invention provides medical application of an ursolic acid-NF (Nuclear Factor)-kappaB inhibitor and relates to application of an NF-kappaB inhibitor as an immunomodifier in the field of medicine and scientific research. As the immunomodifier, the ursolic acid-NF-kappaB inhibitor is used for preparing immunity inhibitor medicines and used in aspects of treating rejection after reducing transplantation and inducing and maintaining transplantation tolerance. As the immunomodifier, the ursolic acid-NF-kappaB inhibitor is used as antiinflammatory drugs and used for treating multiple chronic inflammatory diseases. As the immunomodifier, the ursolic acid-NF-kappaB inhibitor is used for preparing ischemia reperfusion injury protective agents and used for treating ischemia reperfusion injury diseases. As the immunomodifier, the ursolic acid-NF-kappaB inhibitor is used for preparing drugs for preventing and treating endotoxemia and septicopyemia and used for preventing and treating the endotoxemia and the septicopyemia.
EP2563364A1 Combination of carmoterol and fluticasone for use in the treatment respiratory diseases The present invention relates to a pharmaceutical composition comprising carmoterol and fluticasone and/or their pharmaceutically acceptable derivatives as active agents so as to be used in the treatment of respiratory tract diseases, especially in the treatment of asthma and chronic obstructive pulmonary disease (COPD), and the administration of this pharmaceutical composition.
US20080145313 Treatment of cancer by means of RNA interference; compositions comprise small interfering nucleic acid molecule that suppresses expression of target gene involved in energy metabolism pathway within tumor cell, in biosynthesis of nucleotides, in glycogen metabolism, in transport of sugars, amino acids Compositions for the treatment and/or prevention of cancer in a mammal by means of RNA interference are provided, together with methods for the use of such compositions. The compositions comprise a small interfering nucleic acid molecule (siNA) that suppresses expression of a target gene that: (a) is involved in an energy metabolism pathway, such as the glycolysis pathway, within a tumor cell; (b) is involved in the biosynthesis of nucleotides, in glycogen metabolism or is an electron carrier that works with ATP to provide metabolic energy; or (c) is involved in transport of sugars, amino acids, and/or water-soluble vitamins, control of intercellular pH, or drug transport within a tumor cell.
US7649008 Crystal of 4-(1-((4-methylbenzothiophen-3-yl)methyl)benzimidazol-2-ylthio)butanoic acid; has chymase inhibitory activity in living body and can be used as a preventive and/or remedy for inflammatory diseases, allergic diseases, respiratory tract diseases, circulatory diseases, or bone metabolic diseases Various crystal forms of 4-(1-((4-methylbenzothiophen-3-yl)methyl)benzimidazol-2-ylthio)butanoic acid from a solvent, and a process for production thereof are provided.
CA2639285A1 Solid dosage formulations containing weight-loss drugs An orally disintegrating tablet which can be chewed or disintegrated by contact with saliva and containing weight-loss drugs for weight control in humans, especially in children and adolescents, is disclosed.
US20080166404 Contains drugs and stearic acid; post-operative pain Bioadhesive drug formulations that adhere to an oral mucosal membrane of a subject are provided together with single dose applicators and devices for delivering the drug formulations to the oral mucosa, and methods for using the same.
CN103446067A Oxiracetam freeze-drying preparation for injection and preparation method thereof The invention relates to an oxiracetam freeze-drying preparation for injection and a preparation method thereof, belonging to the technical field of medicines. The freeze-drying preparation is a crystal form compound formed by oxiracetam, D-sorbitol and mannitol in a weight ratio of 1: (0.2-0.25): (0.05-0.1). The oxiracetam freeze-drying preparation has the beneficial effects that the production cycle is shortened by about 20 hours, the rate of finished products is increased by above 99%, the phenomena such as the upward shifting and the eruption of the product are avoided, medicine molecules are constrained in crystal lattices, the water content is extremely low and can be controlled below 0.1%, the preparation is difficult to degrade and has relatively good stability, the period of validity is up to 36 months, the impurity content is greatly reduced, the single maximum impurity is less than 0.1%, and the total impurities are less than 0.5%; no organic solvents are involved in the production process, the energy consumption and the cost are substantially reduced, and the technology has environmentally-friendly effect and is suitable for large-scale industrialization production. Compared with the prior art, the oxiracetam freeze-drying preparation provided by the invention has obviously improved curative effect and is suitable for clinical application.
WO2010018217A3 Purin derivatives for use in the treatment of fab-related diseases The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for wound healing preferably in diabetic patients.
US20090281197 Acetic Acid/Thymol Compositions and Their Use in the Treatment of Onychomycosis A composition comprising from about 1 weight part to about 10 weight parts a saturated carboxylic acid having from 2 to about 20 carbon atoms; from about 0.1 weight parts to about 10 weight parts an antifungal compound; and from about 80 weight parts to about 99 weight parts skin-penetrating gel; wherein the saturated carboxylic acid, the antifungal compound, and the skin-penetrating gel together comprise 100 weight parts. In a particular example of the composition, the saturated carboxylic acid having from 2 to about 20 carbon atoms is acetic acid; and the antifungal compound is thymol. A method of treating onychomycosis in a patient, comprising applying the composition. The method provides a safe, effective treatment of onychomycosis.
WO2012138938A1 Aminopyrazine compounds useful as inhibitors of tra kinase The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I): wherein the variables are as defined herein.
CA2678846A1 Peroxisome proliferator activated receptor modulators The present invention is directed to compounds of the structural Formula: wherein: R1 is H or -C1-C3 alkyl; R2 is selected from the group consisting of -H, -C1-C4 alkyl, -C1-C3 alkyl-CF3, phenyl, and pyridinyl; and R3 is selected from the group consisting of -H, -C1-C4 alkyl, -C1-C3 alkyl-O-CH3, -CH2-cyclopropyl, -CH2-C=CH2, -CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; provided that when R1 and R2 are each H, then R3 is selected from the group consisting of -C1-C4 alkyl, -C1-C3 alkyl-O-CH3, -CH2-cyclopropyl, -CH2-C=CH2, -CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; or stereoisomers and pharmaceutically acceptable salts thereof.
EP1940389A2 Modulation of neurogenesis by pde inhibition The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a PDE agent, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.
CA2718676A1 Divalent hydrazide compound conjugates for inhibiting cystic fibrosis transmembrane conductance regulator Provided herein are divalent hydrazide-polyethylene glycol conjugates that inhibit the ion transport activity of a cystic fibrosis transmembrane conductance regulator (CFTR). The conjugates described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea.
WO2012068196A1 Bis heteroaryl inhibitors of pro-matrix metalloproteinase activation This invention relates to thiazole (I) and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
WO2009104198A3 Metal conjugates of indole 3-aldehyde azine and its derivatives and uses thereof Provided are compounds which are metal complexes of indole 3-aldehyde azine and its derivatives, as well as pharmaceutical compositions containing the compounds. Also provided are methods of use of these compounds for preventing or treating a disease such as cancer, caused by one or more conditions such as enhanced angiogenesis, uncontrolled cell proliferation and lack of apoptosis in an animal including human. The method comprises administering to the animal an effective amount of a metal complex of indole 3-aldehyde azine or a metal complex of any of its derivatives.
CN102302504A Application of high-purity baicalin or baicalein to preparation of inhaled asthma relieving medicament The invention discloses application of high-purity baicalin or baicalein to the preparation of inhaled asthma relieving medicaments. The inhaled asthma relieving medicaments comprise the formulations of inhaled solution or inhaled powder sprays, wherein the inhaled solution is prepared from the baicalin or the baicalein and pharmaceutical adjuvants A, and the pharmaceutical adjuvants may be one or more of solvents, latent solvents, surfactants or antioxidants; the inhaled powder sprays are prepared from the baicalin or the baicalein or pharmaceutical adjuvants B, and the pharmaceutical adjuvants B may be one or more of the solvents, the antioxidants or carriers; and the purity of the baicalin or the baicalein is more than 90 percent. Experiments proves that the inhaled asthma relieving medicaments prepared from the high-purity baicalin or baicalein can control the acute paroxysm of asthma effectively, relieve bronchospasm and reduce the resistance of air passages, is high in medicinal effect, small in side effect, nontoxic and low in cost.
US20110077224 Linoleic phospholipids and uses thereof for inhibiting inflammatory and neurodegenerative processes Described herein are compositions of an linoleic phospholipid for inhibiting inflammatory pathways or neurodegenerative processes. Also provided are uses of such compositions and methods of inhibiting inflammatory or neurodegenerative processes by administering a composition that includes an linoleic phospholipid and optionally a carrier to a cell, cell culture or subject in need of such treatment.
US8097263 Silver-containing inorganic antibacterial The present invention provides a silver based inorganic antibacterial agent excellent in heat resistance and chemical resistance, lowered in resin coloring and excellent in processability. The present invention has been completed by finding out that problems can be solved by a silver ion-containing zirconium phosphate represented by the following general formula (1) which is produced by a wet synthesis under specific production conditions. AgaNabHc(H3O)dZreHff(PO4)3 .nH2O (1) wherein, in the formula (1), a, b, c, d, e and f are positive numbers satisfying 1.75<(e+f)<2.25 and a+b+c+d+4(e+f)=9; and n is not more than 2.
US7521451 e.g. 5,6-dimethyl-3a,4,7,7a-tetrahydro-2-benzofuran-1,3-dione;intravenous, water-soluble compounds useful for manufacturing an anasthetic, sedative agents; side effect reduction Provided is a novel isoindoline compound of the formula (I): The compound is useful for anesthesia by inducing sedation in a mammal.
CN103446140A Application of rhynchophylline in preparation of drug with anxiolytic effect and antidepressant effect The invention relates to a drug of indole alkaloid, and particularly relates to application of rhynchophylline in preparation of adrug with an anxiolytic effect and an antidepressant effect. The drug disclosed by the invention is composed of the rhynchophylline and pharmaceutical acceptable auxiliary materials, wherein the content of the rhynchophylline is 1-99.5%. The drug disclosed by the invention is oral preparations and can be tablets, capsules or the like.
US20120208867 Hmgb1 binding nucleic acid molecule and applications thereof A nucleic acid molecule that can bind to HMGB1 protein and applications thereof are provided. A nucleic acid molecule having a dissociation constant for HMGB1 protein of 5×10−7 or less can be used as the nucleic acid molecule that can bind to HMGB1 protein. The HMGB1 binding nucleic acid molecule can bind to HMGB1 protein that is known to be a cause of diseases such as cancer and inflammation, and it is therefore possible to obtain an effect to prevent and an effect to treat such diseases by allowing the HMGB1 binding nucleic acid molecule to bind to HMGB1 protein in a living body.
CN101095759B Medicine that is coated on the navel for treating constipation Disclosed is a medicament for treating constipation through rubbing umbilical part, wherein the raw materials of the active ingredients include dahurian angelica root, bark of peony root, purple perilla, linaloe, boneol.
US20100203144 Immobilized Metallic Nanoparticles as Unique Materials for Therapeutic and Biosensor Applications The present invention relates to compositions and methods by which surface modification techniques can be used to modify wide range polymeric or metal substrates using metal nanoparticles.
US20080027100 Functionally selective alpha2C adrenoreceptor agonists In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
WO2013028049A3 Composition for the percutaneous administration of active compounds providing a suitable treatment for androgenetic alopecia The invention relates to a composition for percutaneous application in a liquid form, comprising minoxidil, tretinoin, clobetasol proponiate and finasteride as the main active ingredients, in addition to a cosurfactant such as diethylene glycol monoethyl ether (Transcutol P) as a potentiator for the application thereof in the treatment of alopecia. The invention also relates to a transporting vehicle, and coadjuvants for the use thereof in the treatment predominantly of androgenetic alopecia.
EP1353692B1 Methods and compositions for treatment of ocular neovascularization and neural injury Methods and compositions for the treatment of ocular neovascularization (CNV) and macular degeneration. The invention includes combining laser treatment with administration of a neuroprotectant.
US20100267653 Use of coumarin derivatives in antifungal therapy The invention provides coumarin compounds, in particular glycosidic coumarin compounds, useful in the treatment of dermatophyte fungal infections.
US20110301130 Topical composition for the treatment of actinic keratosis The invention relates to a topical gel composition for use in the treatment of actinic keratosis comprising (a) an active agent for treatment of actinic keratosis, (b) a keratolytically active agent, (c) a gel former, and (d) an organic solvent.
CN102973663A Toothache treatment aerosol and preparation method The invention discloses a toothache treatment aerosol and a preparation method. The preparation method comprises the following steps: (1) weighing long pepper, clove and borneol; (2) conducting reflux extraction on the long pepper with an ethanol water solution, filtering, recovering ethanol in the filtrate to obtain a thick extract, adding the ethanol water solution, mixing uniformly, standing, and conducting vacuum condensation to obtain an extract 1; (3) extracting clove oil from the clove by a steam distillation method to obtain an extract 2; (4) drying and crushing the extract 1, mixing the dried and crushed extract 1 with the extract 2 and the borneol, dissolving the mixture with the ethanol solution to obtain a propellant solution, packaging the propellant solution into a packaging bottle, and adding a propellant at the pressure of 80-100 bar to obtain the toothache treatment aerosol. The toothache treatment aerosol prepared by the preparation method takes effects quickly, is convenient to take, has remarkable treatment effect, and can address both the symptoms and the root causes, so that the requirements of the majority of patients are met. According to the preparation method, the labor hour is short, and the transfer ratio of active ingredients is high.
CN102085200A New applications of compound mycoE The invention discloses new applications of a compound mycoE and derivatives thereof, which relate to the applications of the compound mycoE and the derivatives thereof to preparing an AMPK (Adenine Monophosphate Activated Protein Kinase) activator and medicines for lowering lipid synthesis and/or enhancing insulin sensitivity and/or lowering glycated protein content in blood serum and/or lowering weight and/or lowering triglyceride content and/or lowering cholesterol content. In the invention, an ELISA (Enzyme-Linked Immuno Sorbent Assay) method is used for establishing a screening model of the AMPK activator to discover the direct and strong activation effect of the mycoE to AMPK. Cell experiments prove that the mycoE can activate the AMPK on a cellular level and lower the lipid synthesis and has extremely low cytotoxicity. Molecular simulation is used for studying the action sites of the mycoE and the AMPK, a site H297 on an AMPK gamma subunit is one of binding sites of the mycoE. Mouse experiments show that the mycoE can obviously enhance the sensitivity of the insulin and lower the glycated protein content in the blood serum, the weight of a mouse and the content of the triglyceride and the cholesterol.
CN101376657A Penem derivative containing sulfhydryl piperidine formyl nitrogen heterocyclic ring The invention belongs to the pharmaceutical technical field, and particularly relates to penem derivatives containing mercaptopiperidinylformylazacyclo, and pharmaceutically acceptable salts, easily-hydrolyzed esters and isomers thereof, shown as a formula (I), wherein R1, R2, R3, R4 and R5 are defined as in the description. The invention also relates to the preparation method of the compounds and a pharmaceutical compound containing the same, and the application thereof on the preparation of pharmaceuticals for treating and/or preventing infection diseases.
US20080138380 Use of Dermatan Sulfrates and/or Desulfated Heparins to Treat or Prevent Heparinoid-Induced Autoimmune Responses Dermatan sulfates and/or O-desulfated heparins useful in treating and preventing heparinoid-induced autoimmune responses, in particular heparin-induced thrombocytopenia (HIT) and its associated disease states. The dermatan sulfates comprise repeating disulfated and/or trisulfated disaccharide units of L-iduronic acid and N-acetyl-D-galactosamine. The O-desulfated heparins comprise heparin molecules selectively O-desulfated at the 2-O and/or 3-O positions of the uronic acid and glucosamine saccharide residues. Particularly effective dermatan sulfate HIT antagonists have a mean molecular weight of from about 2000 to about 10,000 Daltons.
WO2014122067A1 New indanyloxydihydrobenzofuranylacetic acids The present invention relates to compounds of general formula I, (I) wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR 1) and modulate its activity. The compounds are suitable for the treatment and prevention of diseases which can be influenced by this receptor; metabolic diseases, such as diabetes, more specifically type 2 diabetes mellitus, and conditions associated with the disease, including insulin resistance, obesity, cardiovascular disease and dyslipidemia.
CA2756851A1 Therapeutic agent for cancer having reduced sensitivity to molecular target drug and pharmaceutical composition for enhancing sensitivity to molecular target drug Provided are a pharmaceutical composition which enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, wherein the cancer has resistance to the molecular target drug, and a cancer therapeutic agent effective against a cancer having resistance to a molecular target drug, such as gefitinib and erlotinib. The pharmaceutical composition comprising an HGF-MET receptor pathway inhibitor enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, even though the cancer has resistance to the molecular target drug. The cancer therapeutic agent comprising a molecular target drug in combination with an HGF-MET receptor pathway inhibitor is effective against a cancer having resistance to the molecular target drug.
US6872749 Administering to the cow salt of ester of methionine, an ester of methionine amide, and an ester of the hydroxy analogue of methionine The present invention relates to a method for supplying bioavailable methionine to a cow which comprises supplying to the cow an ester of methionine or methionine amide and/or an ester of the hydroxy analogue of methionine or a salt thereof.
US20120045532 Anticancer Methods Employing Extracts of Gleditsia sinensis Lam Selective apoptotic extracts of Gleditsia sinensis Lam are provided. Also provided are methods of using said extracts to induce apoptosis in specific cells, especially in a human. Provided as well are uses of the extracts of Gleditsia sinensis Lam for the preparation of a medicament for the selective induction of apoptosis.
US20080153848 Crystalline Base of Trans-1-((1R,3S)-6-Chloro-3-Phenylindan-1-Yl)-3,3-Dimethylpiperazine Crystalline base of compound trans-1-((1R,3S)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine, processes for the preparation of purified free base or salts of this compound, pharmaceutical compositions comprising the base and medical use thereof, including for treatment of schizophrenia and other psychotic disorders.
CN102988960A Composition which promotes wound healing The invention discloses a composition which promotes wound healing, comprising the components of 0.5-2.5% of chlorhexidine acetate, 1-3.5% of prednisolone acetate, 2-5% of dodecyl dimethyl benzyl ammonium chloride, 0.05-0.3% of vascular endothelial growth factor, 5-15% of sterile water and the balance of ointment matrix by weight percentage. The composition of the invention can obviously shorten the time of wound healing and effectively reduce the width of scar.
EP1463513B1 Stabilized brivudine topical formulations Topical formulations containing the virustatic agent brivudine and stabilizers useful to present its photodegradation are disclosed.
WO2010032269A3 Anti-inflammatory activity of the iridoid glycosides The present invention provides method of treating mammals and humans having inflammation, pain and swelling with pharmaceutical compositions containing iridoid glycosides selected from barlerin. acetyl barlerin and shanzhisidc methyl ester or combination thereof isolated from the plant source or alcoholic extract of the plant source Barleria crislala. Further, the present invention also provides a process for the isolation of these iridoid glycosides.
CN101311174A Vitamin B6 derivates and pharmaceutical use thereof The invention provides a biologically utilizable compound with anti-cancer properties, which is shown as the formula I. The framework of the compound is based on vitamin B6 which is safe to the cells of the human body and is necessary for the human body. The compound can obviously inhibit lung cancer, brain cancer, leukemia and myeloma and has no remarkable inhibition effect or no toxic and side effect on the normal smooth muscle cells of the human body. The invention also provides the composite containing the compound and the pharmaceutic application of the compound.
CN2877688Y Glycyrrhetic acid kali salt thin film coating tablet The utility model discloses potassium glycyrrhefate film-coated tablets, characterized in that a flat and round potassium glycyrrhefate tablet with the diameter between 0.8-1.2cm is used as the tablet base and a coated-film of coat material with the thickness of 0.3-0.9mm is painted on the surface. The coat material adopts moisture proof opadry. The coated-film tablet is small in size, low in cost, moisture proof and stable, improving the disintegration and dissolution rate, the bioavailability, and the clinical effect. The utility model is applicable to the adjuvant therapy for acute and chronic hepatopathy, or to the patients with hepatic dysfunction, and eliminates the restriction for diabetic patients.
CN102755291A Norfloxacin nanometer emulsion used for animals The invention relates to a norfloxacin nanometer emulsion used for animals. The norfloxacin nanometer emulsion comprises the following raw materials in parts by weight: 1-5 parts of norfloxacin, 2-8 parts of acetic acid, 20-40 parts of propylene glycol, 10-20 parts of flaxseed oil, 5-10 parts of polyethylene glycol 400, 10-20 parts of tween, and 10-20 parts of water. The nanometer emulsion has the advantages that the solubility of the norfloxacin in the water is improved, the dispersion degree of the medicine is improved, and the probability that the medicine is connected with an external phase is reduced, so that the bioavailability and stability of the medicine are improved.
CN101933862A Toe cover for preventing and treating foot ulcers The invention relates to a toe cover for preventing and treating foot ulcers, comprising an internal cylinder body (1), an external cylinder body (2) and artificial cotton and medicaments (3). The external cylinder body (2) is arranged outside the internal cylinder body (1); the artificial cotton and the medicaments (3) are filled between the internal cylinder body (1) and the external cylinder body (2); and the medicaments comprises the following components: 0.1 to 0.2 gram of sulfur, 0.1 to 0.2 gram of lightyellow sophora root and 0.1 to 0.2 gram of humifuse euphorbia herb. With respect to the materials, the internal cylinder body and the external cylinder body are made of cloth with air permeability, moisture absorption property and elasticity. For the complete set of technology, the design is artful, two technologies are organically combined and mutually promoted so as to hit the pathogenesis, and the treatment principle of combining treatment and nourishment, including dampness elimination, itch relief and sterilization, is fully embodied.
US20100069479 Neurodegenerative disease treatment using jak/stat inhibition The invention relates to treatment of neurodegenerative diseases with JAK/STAT pathway inhibitors to eliminate extracellular cell signaling events leading to cell cycle abrogation and/or apoptosis. Primary neurons were administered neurotoxic proteins, such as gp120, Tat, or gp120 and Tat, with or without IFN-γ added, resulting in neuronal death, and simulated neurodegenerative diseases. The neurodegenerative disease is treated using a JAK/STAT pathway inhibitor, including (—)-epigallocatechin-3-gallate (EGCG), to modulate JAK1 or STAT1 phosphorylation, resulting in resistance to gp120 or Tat neurotoxicity. The invention may be used to treat neurons afflicted with HIV-associated Dementia, multiple sclerosis, Alzheimer's Disease, Parkinson's Disease, amyotrophic lateral sclerosis, or Pick's Disease, and may act in conjunction with antiviral treatment, like HAART.
US20060216241 Transmucosal absorption through oral mucosa to systemic circulatory system; bioavailability, rapid onset; active ingredient, solvent and low molecular weight hydrocarbon propellant; anxiety, muscle spasms Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide diazepam for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, diazepam, and optional flavoring agent; formulation II: aqueous polar solvent, diazepam, optionally flavoring agent, and propellant; formulation III: non-polar solvent, diazepam, and optional flavoring agent; and formulation IV: non-polar solvent, diazepam, optional flavoring agent, and propellant; formulation V: a mixture of a polar and a non-polar solvent, diazepam, and optional flavoring agent; formulation VI: a mixture of a polar and a non-polar solvent, diazepam, optional flavoring agent, and propellant.
US20080175914 Inflammatory and/or allergic diseases; cognitive impairment The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is C1-4alkyl, C1-3fluoroalkyl, —CH2CH2OH or —CH2CH2CO2C1-2alkyl; R2 is a hydrogen atom (H), methyl or C1fluoroalkyl; R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.
EP1581226A1 Inclusion complex of anti-tubercular rifampicin with beta-cyclodextrin or 2-hydroxypropyl beta-cyclodextrin and a process for producing the same The present invention relates to an inclusion complex of Rifampicin with cyclodextrin as an anti-tubercular drug In addition and also a process for the synthesis of inclusion complexes of the anti-tubercular drug 'Rifampicin' with β-CD and HP-β-CD and characterization of these inclusion complexes.
US6992187 reacting 4,6-dichloro-5-nitropyrimidine with acyclic carboxy amines, then cyclization of the intermediates to form cellular adhesion inhibitors A process for the preparation of a compound of the formula wherein the substituents are defined as in the specification.
CN103242348A Indoline diketopiperazine spiro-compounds as well as preparation method and use thereof The invention belongs to the field of medical and chemical industry, relates to indoline diketopiperazine spiro-compounds as well as a preparation method and use thereof, and in particular relates to compounds as shown in formula I or pharmaceutically acceptable salts of the compounds. The compounds have a framework dimerization molecular structure condensed by terracycloindoline diketopiperazine and 1-oxa spiro[4, 5] decane. Two ethylene oxide structures are arranged on the spiro hexatomic ring. The invention further relates to penicillium purpurogenum for preparing the compounds as shown in the formula I. Experiments show that the compounds can be used for preparing cytoskeletal protein inhibitors, apoptosis inducers, tumor cell proliferation inhibitors, tumor cell killing agents or antitumor drugs. The compounds provided by the invention have good antitumor activity.
WO2013022312A2 Pharmaceutical composition for preventing or treating diabetes or fatty liver containing a cyp4a inhibitor as an active ingredient The present invention relates to a pharmaceutical composition for preventing or treating diabetes or fatty liver, and more specifically relates to a pharmaceutical composition for preventing or treating diabetes or fatty liver containing a CYP4A (cytochrome P450A) inhibitor as an active ingredient. According to the present invention, the CYP4A inhibitor suppresses endoplasmic reticulum stress, reduces the blood insulin concentration and suppresses apoptosis of liver cells, and hence exhibits effects in preventing or treating diabetes or fatty liver.
US20120258918 Polypeptoid pulmonary surfactants The present invention provides spreading agents based on sequence-specific oligomers comprising a peptoid, a peptide-peptoid chimera, a retropeptoid or a retro(peptoid-peptide) chimera, and methods for using the same, including for the treatment of respiratory distress of the lungs. The spreading agents are sequence-specific oligomers, including retrosequence-specific oligomers, based on a peptide backbone, that are designed as analogs of surfactant protein-B or surfactant protein-C.
CN102198119A Externally-applied medicinal patch The invention provides an externally-applied medicinal patch, which comprises an insulation layer, a foam tablet with a certain thickness and a self-bonding function, and a medicinal patch, wherein an accommodating through hole is formed in the middle of the foam tablet; the medicinal patch is arranged in the accommodating through hole; one surface of the foam tablet is adhered on the surface of the insulation layer through a medicinal adhesive; and the other sides of the foam tablets and the medicinal patch are adhered with films. The medicinal patch provided by the invention has high permeability, and the action mechanism of the medicinal patch is advanced and unique; the medicinal patch can be directly adhered on the surface of a body without using adhesive, so the absorption of the medicine is promoted and anaphylactic reactions are reduced; the medicinal patch is fixed by the foam tablet, so the adhesion area with the surface of the body is reduced, allergic reactions are reduced, and the comfort of the patient is enhanced; the foam tablet can absorb body fluid, and the medicinal patch is convenient, quick and sanitary; and the thin films arranged on the outside surfaces of the foam tablet and the medicinal patch can prevent the medicines from violating or being polluted; and the cost of the foam is low and the weight of the foam is light, so the externally-applied medicinal patch is low in cost, simple and practical.
CN103191143A New application of cardiac glycoside compound The invention discloses an application of a cardiac glycoside compound 12 beta-hydroxycalotropin in preparing medicines for treating and preventing tumors. The cardiac glycoside compound 12 beta-hydroxycalotropin has obvious antitumor activity and can be served as a lead compound for treating the tumors. Moreover, an extraction and separation method of the cardiac glycoside compound 12 beta-hydroxycalotropin provided by the invention is simple and practicable and low in cost, and has high efficiency and yield and good extract quality.
US20110251130 Methods and Compositions for Promoting Bone Growth The invention relates to methods and compositions for promoting bone growth, bone healing and/or bone formation. Disclosed herein are isolated truncated Wilms tumor on gene chromosome X (WTX) polypeptides and uses thereof. Also disclosed are methods of treating a bone related disease or condition in a subject by modulating the expression or activity of a (WTX) polypeptide in bone cells of the subject. The bone related disease or condition is any disease or condition including bone related trauma or injury due to any cause including surgery. The compositions and methods according to the invention are useful for enhancing and stimulating bone mineralization and for preferentially directing the differentiation of certain stem cells, thereby altering cell fate.
US20120165405 Anaplerotic Therapy of Huntington Disease and Other Polyglutamine Diseases The present invention relates to a method for treating and/or preventing Huntington disease and other polyglutamine diseases, comprising the step of administering an effective amount of a precursor of propionyl-CoA to an individual in need thereof.
CN103479652A Children's four-vitamin calcium gluconate effervescent tablets and preparation method thereof The invention discloses children's four-vitamin calcium gluconate effervescent tablets and a preparation method thereof. According to the effervescent tablets, vitamin B1, vitamin B2, vitamin C, vitamin D2, calcium gluconate and glucose are taken as raw materials, and total effervescent tablets containing 1000 tablets comprise the following raw materials: 0.4 g of vitamin B1, 0.2 g of vitamin B2, 5 g of vitamin C, 140 thousand units of vitamin D2 calculated according to 40 thousand units/mg, 300 g of calcium gluconate, 300 g of glucose, and 80%-60% by weight of auxiliary materials accounting for the total tablets. The children's four-vitamin calcium gluconate effervescent tablets are prepared by a special technology, and are good medicine for supplementing vitamins and calcium in children bodies as a vitamin and calcium supplement medicine; and the children's four-vitamin calcium gluconate effervescent tablets have the characteristics of being high in bioavailability, good in mouthfeel, convenient to use, easily accepted by children, convenient to carry and the like. Because of the auxiliary materials and the annular effervescent tablets, the children's four-vitamin calcium gluconate effervescent tablets can be rapidly disintegrated.
US20110060005 Treatment of mitochondrial disorders using a farnesyl transferase inhibitor Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies and mitochondrial disorders are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject an amount of a farnesyl transferase inhibitor, wherein the amount administered is sufficient to stimulate mitophagy in said subject. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant.
CN1575796A Ligustrazine phosphate dripping pill and preparation thereof The present invention relates to one kind of medicine for treating obliterative vascular disease, cerebral thrombosis, angitis, coronary heart disease, etc. and its preparation process. The present invention provides chuanxiongzine dripping pill with high bioavailability, fast release and acting, no toxic side effect and convenient carrying about. The chuanxiongzine dripping pill is prepared with chuanxiongzine hydrochloride as main material, and through adding surfactant polyglycol-6000 and other matrix in certain proportion, mixing, heating to smelt, stirring and dropping into condensate in special dripping pill machine.
CN1799539A Compound glutamine granules and preparation method thereof The invention discloses a compound glutamine granule and its preparing process, which consists of coating sodium azulene sulfonate with beta-cyclodextrin to obtain sodium azulene sulfonate inclusion compound, then mixing the inclusion compound with L-glutamine homogeneously, charging 3 wt% of carboxymethyl cellulose solution, stirring homogeneously to obtain soft material, finally granulating the soft material.
WO2011150453A1 Diagnostic, prognostic and therapeutic use of a long non-coding rna In alternative embodiments, this invention relates to the use of a long non-coding anti-sense RNA for the diagnosis, prognosis and therapy of cancer, including breast cancer. The invention also relates to the design and production of therapeutic agents that modulate ZFAS1 expression and/or activity. The therapeutic agents may be used to modulate abnormal cell proliferation and/or alleviate symptoms associated with the development and/or progression of cancer.
EP2575827A2 Urea sorbent A sorbent polymer is provided that interacts or reacts with aqueous urea to aid the regeneration of a dialysate liquid. The sorbent polymer may include one or more specific functional groups bonded thereto. Such specific functional groups are selected from carboxylic acids, carboxylic acid esters, carboxylates, amides, dicarboxylic acids, dicarboxylic acid esters, and dicer boxylates to produce the desired urea sorbent.
CN101805384A Novel lycoris quinolone alkaloid and preparation method and application thereof The invention belongs to the technical field of the natural drug, and discloses a chemical structure of a novel lycoris quinolone alkaloid extracted and separated from a lycoris plant atamasco. The compound is of a structure as shown in the formula on the right. The invention also discloses a preparation method and application of the compound in the field of medicine, in particular the application in preparation of anti-tumor drugs for treatment of leucocythemia and the like.
EP1175205B1 Solid dispersion comprising ritonavir, fenofibrate or griseofulvin A pharmaceutical composition is disclosed which comprises a solid dispersion of a pharmaceutical compound in a water soluble carrier, such as polyethylene glycol (PEG), and a crystallization inhibitor, such as polyvinylpyrrolidone or hydroxypropylmethylcellulose. The solid dispersion may optionally be encapsulated in hard gelatin capsules, compressed into a tablet, or may be granulated wiht a pharmaceutically acceptable granulating agent. Also disclosed are methods of making said solid dispersion and methods of treatment employing said solid dispersion.
CN101361978A Anti-cancer medicine release system using cellular membrane biomimetic modification polyamide-amide as carrier and preparation method thereof The invention discloses an anti-cancer drug delivery system adopting polyamide-amine modified by cell membrane in a bionic manner as a vector, and a preparation method thereof. A Michael addition reaction between an amido polyamide-amine arborization polymer which is an outer layer and a cell membrane bionic monomer is utilized for realizing surface modification of the polyamide-amine so as to obtain the polyamide-amine modified by the cell membrane in a bionic manner. The polyamide-amine modified in a bionic manner has a hydrophobic cavity and a hydrophobic interaction between a hydrophobic anti-cancer drug and the hydrophobic cavity, thereby realizing the embedding of the anti-cancer drug in the polyamide-amine modified by the cell membrane in a bionic manner. A formed complex of the polyamide-amine and the anti-cancer drug can realize the effective delivery of the anti-cancer drug. The invention has comparatively high drug effects and drug-loading capacity, excellent water solubility and storage stability as well as comparatively low toxicity, thereby having good application prospect in the treatment of cancers.
US20060148896 Use of an alkanoyl L-carnitine for the preparation of a medication to treat anhedonia The present invention relates to the use of an alkanoyl L-carnitine, or pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of anhedonia.
EP1793832A2 Geranylgeranyl pyrophosphate synthase inhibitors The invention provides novel pyrophosphate synthase inhibitors of formula (I), wherein R1 is a saturated or unsaturated: (C5-C20)alkyl chain that optionally comprises one or more aryl rings in the chain and that is optionally substituted with one or more halo, trifluoromethyl, -ORa, -P(=O)(ORa)2, or -NRbRc; R2 is a saturated or unsaturated (C5-C20)alkyl chain that optionally comprises one or more aryl rings in the chain and that is optionally substituted with one or more halo, trifluoromethyl, -ORa, -P(=O)(ORa)2, or -NRbRc; R2; each R3, R4, R5, and R6 is independently OH or (C1-C6)alkoxy; each Ra is independently H, (C1-C6)alkyl, or aryl; and .each Rb and Rc is independently H, (C1-C6)alkyl, or aryl; or Rb and Rc together with the nitrogen to which they are attached form a pyrrolidino, piperidino, morpholino, or thiomorpholino ring; wherein any aryl is optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NRdRe, or S(O)2NRdRe, wherein each Rd and Re is independently H or (C1-C6)alkyl; or a pharmaceutically acceptable salt or prodrug thereof. Also provided are compositions comprising such inhibitors and methods for their use.
US20100130574 Neurodegenerative diseases and methods of modeling This invention relates to methods for neuroprotection, promoting survival of motor neurons and the treatment of motor neuron diseases by preventing cell signaling through the classic prostaglandin D2 receptor DP1.
WO2008148867A3 Quinoxaline derivatives as inhibitors of the tyrosine kinase activity of janus kinases The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R; R2 is caryl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8 R3, R4, and R5 are each independently hydrogen or R9; R6 is hydrogen; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases.
US20110236502 Vitamin Strip (V1) The vitamin strip is made with gel, film, or dissolvable material safe for human consumption. It can encompass all the vitamins, minerals, medicines, or meal replacement elements safe for human intake. The vitamin strip (V1) can be made as a whole or as a strip of edible dissolvable material with any vitamin(s), mineral(s), medicine(s), or meal replacement element(s) safe for human consumption on the strip of edible dissolvable material.
EP2621926A2 Pyrazolopyrimidine pde10 inhibitors The present invention is directed to pyrazolopyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
WO2006081739A1 A composition for treating or preventing hyperlipemia, hypertension and hepatic adipose infiltration A composition for treating or preventing hyperlipemia, hypertension and hepatic adipose infiltration. The composition is prepared by using following weight proportion of raw material drugs including 5-60 parts of Monascus purpureus Went, 0.3-50 parts of soy isoflavone, 10-75 parts of rhizoma of Alisma plantago-aquatica L. var. Orientale Samuels, as well as optional one of Fructus of Crataegus pinnatifida Bge. var. Major N. E. Br., Crataegus cuneata Sieb. Et Zucc., Crataegus pinnatifida, Crataegus hupensis Sarg., Crataegus Pall., Crataegus scabrifolia (Franch.) Rehd. or Semen of Cassia tora L. or both. The composition according to the present invention have no toxic side effect, and have good effects on regulating fat, can significantly reduce cholesterol, triglyceride, low density lipoprotein in the blood, have apparent effects on treating and preventing hypertension, hepatic adipose infiltration, and can be used in preparing drugs or health foods for treating and preventing hyperlipemia, hypertension and hepatic adipose infiltration.
CN103006635A Application of brazilin to preparation of drug or health care product for inhibiting aggregation of beta-amyloid proteins The invention discloses an application of brazilin to preparation of drug or a health care product for inhibiting aggregation of beta-amyloid proteins. Various experimental means prove that brazilin can inhibit amyloid beta 42 aggregation, can change the appearance of the amyloid beta 42 aggregation, prevents and slows down the conversion of the appearance of the amyloid beta 42 aggregation into the fibrous appearance, slows down the process of converting a secondary structure of the amyloid beta 42 into a beta-sheet structure, decreases the content of the amyloid beta 42 converted into the beta-sheet in the solution, and inhibits the amyloid beta 42 aggregation from producing a toxic effect on cells effectively. Brazilin is considered as a potential new rug or health care product molecule, can inhibit amyloid beta 42 aggregation effectively and the comformational change process of the amyloid beta 42 aggregation, reduces the cytotoxic effect generated during the amyloid beta 42 aggregation process, and is an ideal inhibitor for amyloid beta 42 aggregation.
CN102659840A Imidazole diphosphonie acid compound and pharmaceutically-acceptable salt and medicinal application thereof The invention relates to a novel imidazole diphosphonie acid compound and a pharmaceutically-acceptable salt thereof. The diphosphonie acid compound disclosed by the invention, farnesylpyrophosphate synthetase is treated, and lipotropy is enhanced. The type of compound can be used for treating diseases including osteoporosis, hypercalcinemia and the like, and can be applied to cancer chemotherapy, immunotherapy and the like.
CN1919339A Cucurbitacin nano preparation comprising protein, preparation method and use thereof The invention discloses a cucurbitacin nanometer agent with protein, which can be liquid agent or solid agent. The protein nanometer particle can be reserved under indoor temperature, which improves drug quality and effect. the liquid agent contains0.05-10% (W/V) protein quantity and 0.001-1% (W/V) cucurbitacin and the solid agent consists of 50-99.9% (W/V) protein and 0.001-50% (W/V) cucurbitacin.
US20060166940 Such as (R)-2-amino-2-methyl-4-[4-(4,4,5,5,5-pentafluoro-pentyloxy)-phenyl]-butan-1-ol hydrochloride for treatment of disorders or diseases mediated by lymphocytes, and for treating acute or chronic transplant rejection or T-cell-mediated inflammatory or autoimmune diseases Compounds of formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
DE102005057421A1 New heteroaromatic sulfonamide prodrugs, useful for delivering e.g. antimalarials and steroids for e.g. fertility control or hormone replacement therapy Sulfonamide prodrugs (I) are new. Sulfonamide prodrugs of fromula (I) are new Drug-OCO-X-SO2NH2 (I) X : optionally substituted heteroaromatic group or alkyl-heteroaromatic group; Drug : pharmaceutical able to form a carboxylate ester through an hydroxy group, such as steroids, antimalarials, nucleosides, isoflavonoids, optionally substituted . An independent claim is included for methods for preparing (I). - ACTIVITY : Contraceptive; Antiinfertility; Cytostatic; Gynecological; Antiinflammatory; Antiallergic; Protozoacide. - MECHANISM OF ACTION : Inhibition of carboanhydrase (CA). The compound 3-hydroxyestra-1,3,5(10)-trien-17beta -yl 6'-sulfamoylnicotinate has ID50 against human CAI and CAII of 2900 and 31 nM, respectively.
WO2006121467A3 Tetrahydrocarbazole derivatives for treating flaviridae viruses The present invention relates to compounds that are useful in the treatment of viruses belonging to Flaviviridae, including flaviviruses, pestiviruses, and hepaciviruses. The invention includes compounds useful for the treatment or prophylaxis of dengue fever, yellow fever, West Nile virus, and HCV.
CN1939259A Oral preparation containing penicillin G and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains penicillin G. Its preparing process is also disclosed.
EP2222668A1 Tetrahydrocyclopenta[b]indol-3-yl carboxylic acid derivatives useful in the treatment of autoimmune and inflammatory disorders The present invention relates to certain (1,2,4-oxadiazol-3-yl)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl carboxylic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
US20120035246 Single-stranded nucleic acid molecule having nitrogen-containing alicyclic skeleton Provided is a novel nucleic acid molecule that can be produced easily and efficiently and can inhibit the expression of a gene. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes: a region (X); a linker region (Lx); and a region (Xc). The linker region (Lx) is linked between the regions (Xc) and (Xc). The region (Xc) is complementary to the region (X). At least one of the regions (X) and (Xc) includes the expression inhibitory sequence. The linker region (Lx) has a non-nucleotide structure including at least one of a pyrrolidine skeleton and a piperidine skeleton. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.
US20120157525 Treating eczema and/or psoriasis The treatment of humans or other mammals for eczema and/or psoriasis using dosage forms or compositions that include cetyl myristate alone or (in admixture or serially) both cetyl myristate and cetyl palmitate.
CN102670519A Quickly-dissolvable dienogest oral preparation and preparation method thereof The invention belongs to the field of pharmacy, and particularly relates to a quickly-dissolvable dienogest oral preparation and a preparation method thereof. The technical problem to be solved of the invention is to provide a quickly-dissolvable dienogest oral preparation, which can be used for realizing quick dissolving of dienogest by over 95 percent within 5 minutes to fulfill the aim of quick response. The dienogest oral preparation consists of dienogest and medicinal auxiliary materials, and is characterized in that: the particle diameter of the dienogest is 15-50 mum; and the medicinal auxiliary materials are common medicinal auxiliary materials for preparing the oral preparation. The invention provides a quickly-dissolvable dienogest oral preparation and a preparation method thereof. A product has reliable quality, is safe, and can act quickly; and moreover, the preparation method is simple and practicable, and contributes to industrial production.
US7422756 Mixture of fatty acid and cholesterol The invention concerns a skin preparation for moistening human skin comprising a combination of a component A and a component B, wherein A includes at least two saturated C9-C31 fatty acids selected from the group consisting of iso- and anteiso fatty acids, whereby component B consists of cholesterol in an amount of 5-15% by weight of component A.
CN101701018A 2-(4-aminoquinazoline) benzo [d] thiazole derivative and application thereof The invention relates to a 2-aminobenzo [d] thiazole derivative with a structure of the formula (I), a pharmaceutically acceptable salt and an application thereof. Proved by pharmacological tests, the compound or the pharmaceutically acceptable salt thereof has an inhibiting effect on the proliferation of various tumor cells.
CN103127342A Ointment capable of curing scald and preparation method thereof The invention discloses ointment capable of curing scald. The ointment capable of curing the scald is characterized in that the components of the ointment comprises gamboge, artemisia anomala, frankincense, daemonorops draco, radix angelicae, angelica sinensis, Chinese goldthread, borneol, sanguisorba officinalis, cortex lycii radicis, and gypsum rubrum. The invention further provides a preparation method of the ointment capable of curing the scald. The preparation method of the ointment capable of curing the scald includes that appropriate amount of the gamboge, the artemisia anomala, the frankincense, the daemonorops draco, the radix angelicae, the angelica sinensis, the Chinese goldthread, the borneol, the sanguisorba officinalis, the cortex lycii radicis, and the gypsum rubrum are chosen, added into a steel barrel with a cover, immersed into good quality sesame oil, after being immersed for a few days, placed on a stove, first heated by soft fire and then heated by strong fire. When the leaves are crunchy, the leaves are pulled out, then the strong fire is changed into small fire, while the components are hot, the borneol and appropriate amount of the Chinese goldthread are added and agitated continuously to speed up the melt, after the components are cooled, the applicable ointment is obtained. An atrauman application method is used by the ointment, not only are patients provided with convenience, but also the treatment is not affected, the curing rate is improved, and the frequency of dressing change can be decided by wound exudation and pain size of a patient.
CN101380294A Preparation method of solid dispersion medicine for treating hemorrhage The invention relates to a method for preparing a solid dispersion medicine for treating hemorrhagic disease. The solid dispersion medicine for treating the hemorrhagic disease is prepared according to the parts by weight as follows: 1-5 parts of dencichine, 0.4-2 parts of a cosolvent, 0.5-2.5 parts of a dispersion carrier and 0.1-0.5 part of a cryoprotectant. The invention also discloses a method for preparing the solid dispersion medicine and a method for preparing the solid dispersion medicine into various pharmaceutically acceptable dosage forms by adding pharmaceutic adjuvants, such as injection, oral solid preparation and preparations for external use. The solid dispersion medicine has obvious functions of preventing and treating hemorrhage. The medicine is prepared by a dispersion system and better disperses both in vivo and in vitro, which is beneficial to the absorption of human body, thus improving the haemostatic effect.
US20100143505 Indanone inhibitors of acetylcholinesterase The present invention relates to new indanone inhibitors of acetylcholinesterase, pharmaceutical compositions thereof, and methods of use thereof.
CN103204774A Ibuprofen compound and pharmaceutical composition thereof The invention belongs to the technical field of medicines, and particularly relates to an ibuprofen compound. The structure formula of the ibuprofen compound is shown in the specification. An X-ray powder diffraction spectrum of the Ibuprofen compound measured by a Cu-K alpha ray is shown in figure 1. A preparation method of the ibuprofen compound and a pharmaceutical composition containing the ibuprofen compound are also provided by the invention. The ibuprofen pharmaceutical composition is ibuprofen injection and Ibuprofen sterile powder injection. Compared with the prior art, the ibuprofen compound and the pharmaceutical composition thereof provided by the invention have better storage stability; and the medication safety of a sufferer is greatly improved.
CN101138542A Lidocaine hydrochloride partial film forming gel composition and uses thereof The present invention discloses a compound of an lidocaine hydrochloride local membrane forming gel, which comprises the components of the following weight percentages comprising the 0.5 percentage to 7 percentage of alkyl cellulose, 1 percentage to 10 percentage of etherifying agent, 0.5 percentage to 5 percentage of cross linking agent, 75 percentage to 90 percentage of dissolvent , 0.1 percentage to 5 percentage of lidocaine hydrochloride . The cross linking agent is the saturated fat or the alcoholic acid, the chemical general formula of which is CnH2n+2-m-l(OH)m(COOH)l. Among the formula, m or n or 1 is the integer and the n is no less than m which is no less than 2. 1 is no less than 0 and the result of m plus 1 is 4 to 8. The result of n plus 1 is 4 to 8. In the present invention, the compound of the lidocaine hydrochloride local membrane forming gel is applied in the treatment of the local pain relieving in the tissue of the skin or the mucosa. A water drain protective membrane with smooth property, firm property, wear-resisting property and duration property is formed on the surface of the ulcer when the present invention is applied. Compared with all kinds of local formulation of the lidocaine hydrochloride, the membrane formed by the gel compound is not likely to experience fracture, dissolution or corrosion. The membrane can be effectively maintained in the mouth mucosa surface for over 5 hours and the membrane can be effectively maintained on the skin surface for over 8 hours.
EP2079474A1 Liposome encapsulated poly-iclc method to prophylactically treat an avian influenza viral infection A method of treating an avian influenza viral infection using a poly ICLC formulation with improved therapeutic efficacy is disclosed. The poly ICLC is encapsulated within liposomes which provides a drug delivery system with slow sustained release characteristic and which has the ability to target the drug to sites of viral infection without causing systemic burden to normal tissues, thereby enhancing the immunological and biological activities of poly ICLC. This poly ICLC formulation has been found to be particularly effective in treating an avian influenza viral infection and in particular, an avian H5N1 influenza viral infection.
US20080312143 Modified Cdna for High Expression Levels of Factor VIII and Its Derivatives The present invention relates to modified DNA sequences coding for biologically active recombinant human factor VIII and its derivatives, recombinant expression vectors containing such DNA sequences, host cells transformed with such recombinant expression vectors, and processes for the manufacture of the recombinant human factor VIII and its derivatives. The invention also covers a transfer vector for use in human gene therapy which comprises such modified DNA sequences. The present invention relates to modified DNA sequences coding for biologically active recombinant human factor VIII and its derivatives, recombinant expression vectors containing such DNA sequences, host cells transformed with such recombinant expression vectors, and processes for the manufacture of the recombinant human factor VIII and its derivatives. The invention also covers a transfer vector for use in human gene therapy which comprises such modified DNA sequences.
WO2014092589A1 Process for preparation of prasugrel hydrochloride polymorphic form b of pharmaceutical purity Process for preparation of prasugrel hydrochloride polymorphic form B of phannaceutical purity is characterized by that addition reaction of prasugrel base and hydrochloride is carried out in an organic solvent selected from a group comprising ketones, aliphatic ester, and aliphatic or cyclic ethers, with the addition of methyl alcohol at 0.1 -10% volume in relation to the volume of solvent used in the reaction, and seed crystals of prasugrel hydrochloride polymorphic form B.
WO2006092024A1 Compounds having anti-cancer properties There is provided a method for alleviating symptoms, treating or preventing cancer, the method comprising administering to a subject, having or at risk of developing cancer, a pharmaceutical formulation comprising an effective amount of one or more phosphate derivatives of one or more hydroxy chromans selected from the group consisting of 7:8 dimethyl 6 hydroxy chromans, 8 methyl 6 hydroxy chromans and mixtures thereof.
US20100292339 Genetic Polymorphisms Predictive of Nutritional Requirements for Choline in Subjects Methods of predicting susceptibility of a subject to develop one or more choline deficiency-associated health effects are provided, comprising determining a genotype of the subject with respect to at least one choline metabolism gene and comparing the genotype of the subject with at least one reference genotype associated with susceptibility to develop the one or more choline deficiency-associated health effects.
CN103070868A IDO inhibitor containing NH-1,2,3-triazole and preparation method thereof The invention belongs to the technical field of drug synthesis, and particularly relates to an IDO inhibitor containing NH-1,2,3-triazole and a preparation method thereof. According to the method, antitumor drug Erlotinib containing acetenyl is used as a raw material to react with azidotrimethylsilane or toluene sulfonyl azide under the catalysis of a cuprous compound, then a NH-1,2,3-triazole group is inducted to synthesize the novel IDO inhibitor containing NH-1,2,3-triazole. According to the invention, the novel NH-1,2,3-triazole synthesized through the method can be used as a high efficiency IDO inhibitor, and can be applied to diseases provided with tryptophane metabolic pathway pathology characteristics mediated by the IDO; and the diseases at least comprise tumor disease, cancer, Alzheimer disease, autoimmunity disease, cataract, mood obstacle, depression and anxiety disorder. According to the invention, the method has the advantages of simplicity in operation, mild condition, low cost, high yield, and expansive application prospect, and is easy for industrialized production.
WO2009023903A1 Compositions comprising phospholipids The present invention provides compositions comprising phospholipids and particularly those comprising at least 40% phospholipid and at least 80% phospholipid as a percentage of total fat in the extract, comprising polyunsaturated and saturated phospholipids, in a ratio of saturated phospholipid to monounsaturated to polyunsaturated phospholipid of about 6:3:1 respectively, or comprising at least 40% phospholipid and less than 40% protein and methods for their production from dairy products.
CN101161235A Dasatini sustained-release implants for treating entity knub A dasatinib slow release implant for treating solid tumor is characterized in that the slow release implant contains anti-cancer effective amount dasatinib, slow release supplementary materials and some slow release regulator. The solid tumors comprise lung cancer, esophagus cancer, stomach cancer, liver cancer, breast cancer, ovarian cancer, prostatic cancer, bladder cancer and colorectal cancer. The slow release supplementary materials mainly are one or their combination of co-polymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate), and poly (L-lactide-co-propyl phosphate), during its degradation and absorption, slow releasing dasatinib to tumor local, so it greatly decreases its whole body toxicity reaction, at the same time it also maintains effective medicine concentration of tumor local. The tumor local is arranged with the slow release implant, which can not only decrease whole body toxicity reaction of dasatinib, but also selectively promote medicine concentration of the tumor local, reinforce therapeutic effect of non-operation therapy such as chemotherapeutic drugs, radiotherapy and etc.
WO2009021325A1 Microrna compositions and methods for the treatment of myelogenous leukemia The invention provides methods, uses, kits and compositions comprising a therapeutically effective amount of the microRNA miR-223 for treating myelogenous leukemia in a subject in need of such treatment. The invention further comprises methods encompassing the use of miR-223 for promoting the differentiation of a leukemia stem cell that is resistant to a differentiating agent, and a method of screening for candidate compounds capable of treating a myeloid leukemia by comparison of the therapeutic activity of the candidate compound with the therapeutic activity of miR-233.
CN101385726A Use of alpha-lipoic acid in preparing medicine or food for improving senile memory The invention relates to the use of Alpha-lipoic acid in the preparation of drugs or foods for improving the memory of elderly people. The experiments confirm that the Alpha-lipoic acid can significantly improve the passive avoidance ability, the active avoidance ability and the space memory exploration ability by being given to senile mice, thereby having the effect of improving the memory of the elderly people.
US20100330098 Methods to regulate glucose metabolism The present disclosure describes an unexpected and novel insight into hepatic insulin resistance through the description of the ability of VEGF inhibitors to revert hyperglycemia and hyperinsulimenia in murine Type 2 diabetes mellitus models through modulation of a HIF-2α-IRS-2 axis operative in hepatocytes. As such, the data of the present disclosure uncover a novel pathway regulating hepatic IRS-2 expression, and identify VEGF inhibitors as an FDA-approved class of therapeutics capable of increasing liver IRS levels and ameliorating Type 2 diabetes mellitus. Accordingly, this disclosure identifies stabilization of HIF-2α as a robust method for improving glucose metabolism. The disclosure provides embodiments of a method of modulating the level of glucose metabolism of a mammalian cell, comprising: contacting a mammalian cell with an effective amount of a composition, where the composition can modulate the levels of HIF-2α and IRS-2 activity in said cell, thereby modulating the level of glucose metabolism by said cell. The disclosure also provides embodiments of a pharmaceutical composition and methods for their use for the treatment of Type 2 diabetes in an animal or human subject, the method comprising administering to an animal or human subject a effective amount of a pharmaceutically acceptable composition, the composition, when administered to an animal or human subject, increasing the activity of HIF-2α and IRS-2 in the animal or human subject, thereby reducing the level of blood glucose in the animal or human subject.
WO2013115486A1 Novel piperine derivative and use therefor The present invention relates to a novel piperine derivative. The present invention provides a pharmaceutical composition or functional food composition which comprises a piperine derivative as an active ingredient, and which is for preventing or treating a metabolic disorder selected from the group consisting of obesity, diabetes, dyslipidaemia, fatty liver and insulin resistance syndrome. The piperine derivative of the present invention can advantageously be used as a medical or functional food composition which suppresses the differentiation of adipocyte precursor cells and reduces the amount of triglycerides accumulated in cells and so ultimately exhibits an action in preventing or treating a metabolic disorder selected from the group consisting of obesity, diabetes, dyslipidaemia, fatty liver and insulin resistance syndrome.
CN1796419A Dressed and modified sugar of monosaccharide/disaccharide This invention publishes a modification of monosaccharides and/or disaccharides with modifiers and the modified saccharides. It further publishes the preparation method for the modified saccharides and their application in dietary fibers, anti-obesity drugs and health products. This invention enlarges the application of monosaccharides and disaccharides and promotes their exploitation value. It has the advantages of simple preparation, facile raw materials and low cost and is thus of great industrial practicability.
US20120301548 Oral complex composition comprising pseudoephedrine and levocetirizine An oral complex composition which comprises (i) a core comprising a swellable hydrogel-forming agent and pseudoephedrine, or a pharmaceutically acceptable salt thereof; (ii) a first coating layer encasing the core which comprises a water-soluble substance; and (iii) a second coating layer deposited on the first coating layer which comprises levocetirizine or a pharmaceutically acceptable salt thereof together with polyvinylalcohol, povidone, polyvinylalcohol-polyethyleneglycol graft copolymer or a mixture thereof, has an improved levocetirizine releasing rate and does not show a delayed release behavior even after a long storage period. Accordingly, the inventive oral complex composition is useful for treating perennial or seasonal allergic diseases including nasal obstruction, sneezing, and rhinorrhea.
EP2731585A1 Cosmetic and/or dermatological use of oligosaccharide compounds for preventing and treating stretch marks The present invention relates to a topical composition, in particular a cosmetic and/or dermatological composition, to be used for preventing and/or treating stretch marks, including, in a physiologically acceptable medium, an effective amount of at least one synthetic polysulfated oligosaccharide having 1 to 4 glycose units, the salts thereof, and/or the derivatives thereof. The invention also relates to a cosmetic method, in particular for treating stretch marks, including at least one step of applying said composition to the skin.
CN102151285A Neutral calcium supplement preparation The invention provides a neutral calcium supplement preparation which has the main components by weight: calcium carbonate powder and citric acid according to the proportion of 9.5-10.5: 1; and preferentially, the proportion between the calcium carbonate powder and the citric acid is 10: 1. The neutral calcium supplement preparation is simple and reasonable in components as well as efficient and safe in calcium supplement effect, and has supplementing, treating and health care functions for preventing calcium deficiency and diseases caused by calcium deficiency.
CN102824382A Method for preparing Ligusticum wallichii lactone extract having anti-liquid-accumulation activity, and use The invention relates to a method for preparing Ligusticum wallichii lactone extract having anti-liquid-accumulation activity and a use, especially to a Ligusticum wallichii extract containing 30 to 90 % of ligustilide. The extract is prepared by the following method comprising smashing the Ligusticum wallichii medicinal materials, immersing in 70 to 99 % ethanol, e.g. 75 to 98 %, extracting by reflux for 1 to 4 times, combining extract, condensing, extracting by using petroleum ether, recovering the solvent of the combined extract till dryness to get a petroleum ether extract; extracting a part of the extract by using the petroleum ether, adding normal phase silica gel to stir, going through a normal phase silica gel column, eluting by using the petroleum ether and an ethyl acetate solution with a volume ratio of 50 : 0.5-5 as eluents, collecting the eluates, and condensing to get the Ligusticum wallichii lactone extract.
US7709451 Method and composition for treating immune complex associated disorders The present invention provides methods and compositions for treating immune complex associated diseases (ICAD), such as SLE, rheumatoid arthritis, and hepatitis-C related immune complex disease (e.g., cryoglobulinemia) in a subject having an ICAD or at risk for developing ICAD. The invention is based upon the surprising finding that chromatin-containing immune complexes activate autoreactive B cells and dendritic cells by a dual receptor engagement process which, in both cell types, involves a Toll-like receptor (TLR). The methods of treating ICAD comprise administering a compound to an individual in need thereof that either 1) inhibits formation of the immune complex either by preventing formation and/or binding to the TLR, or 2) interferes with binding of an autoantigen-containing immune complex (or the antigenic component thereof) to the TLR, or 3) inhibits signaling pathways initiated by dual engagement of BCR and TLR (in B cells) or FcR and TLR (in dendritic cells) via immune complexed or uncomplexed autoantigens.
WO2006089781A1 Pharmaceutical combination of bcr-abl and raf inhibitors The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) a RAF kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination, wherein compound a) has the following general Formula: (I).
CN101810845A Nutritional agent for enhancing immunity, restoring gastrointestinal function and protecting heart, brain, liver and kidney cells The invention discloses a nutritional agent for enhancing immunity, restoring a gastrointestinal function and protecting heart, brain, liver and kidney cells. The nutritional agent comprises the following raw materials in part by weight: 3 to 28 parts of ganoderan powder, 2 to 49 parts of protein powder, 1 to 24 parts of maitake extract and 4 to 22 parts of compound lactobacillus. The nutritional agent has the following advantages of remaining nutrients and active ingredients in each component of the raw materials to the maximum, supplementing various nutrients and proteins for a human body, and having the effects of anti-blood lipid, anti-blood glucose, anti-virus, anti-genetic mutation, anti-tumor, anti-radiation, liver-protection, anti-fatigue, gastrointestinal mucosa restoring, and the effect of helping to restore damaged heart, brain, liver and kidney cells of the human body.
WO2005041931A3 Pharmaceutical aerosol compositions Disclosed are metered dose inhalers having a metering valve to deliver a dose containing an aerosol suspension formulation, said aerosol suspension formulation comprising: an effective amount of Mometasone Furoate, Formoterol or a combination thereof; a suspension medium selected from the group consisting of 1,1,1,2,3,3,3,-heptafluoropropane, 1,1,1,2-tetrafluoroethane; and a solvent that is ethanol; wherein said formulation contains less than about 500 µg of non-volatile residue as measured by ultraviolet spectroscopy.
US20120201822 Tumor treatment The invention concerns an improved method for treating tumor, including cancer, which combines the administration of a chemotherapeutic agent and an antagonist of a gene product the expression of which is upregulated by the chemotherapeutic agent. The invention further concerns methods and means for the diagnosis and classification of tumors, and for the prognosis of the outcome of tumor treatment, and patient response to a particular treatment modality.
EP2276722A2 Polymorphic form of an aminoindan mesylate derivative The invention relates to a polymorphic form of rasagiline mesylate, and to processes for preparing the same.
EP1267826B1 Pharmaceutical composition for treatment of mucosal epithelial ulceration and/or erosion A bioadhesive pharmaceutical composition for treatment of mucosal epithelial ulceration and/or erosions, said composition comprising: (i) a bioadhesive substance; (ii) a biologically active substance having MMP inhibitory activity; and (iii) an optional physiologically acceptable vehicle; said bioadhesive substance and optional physiologically acceptable vehicle being selected to release the biologically active substance in a therapeutic amount into the epithelia of the mucosa without affecting the normal flora thereof; use of the composition for the manufacture of a medicament for treating mucosal ulceration and/or erosion; a method of treating mucosal epithelial ulceration and/or erosion in a mammal; and a method of delivering a biologically active substance to the mucosa of a mammal for treatment of mucosal epithelial ulceration and/or erosion.
WO2012165736A1 Remedy for gastritis and gastric ulcer The present invention relates to processing bay salt and bamboo trees into a heat-treated salt having a purple color and developing same into a remedy for gastritis and gastric ulcer. The method for manufacturing the remedy comprises a step of preliminarily heat-treating the bay salt containing abundant minerals with bamboo trees at a temperature of at least 1100℃, and repeatedly heat-treating the salt that is preliminarily heat-treated with bamboo trees under the same condition to manufacture a heat-treated salt containing a significant amount of hydrogen sulfide and having the purple color. The heat-treated salt, when used with aspirin, among others, shows superior effectiveness in preventing damage to the stomach, such as significantly reducing hemorrhage, ulcers, and mucosa damage induced from aspirin use.
WO2005030212A1 4-aminoquinoline-3-carboxamide derivatives as pde4 inhibitors Compounds of formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.
WO2010032704A1 Pharmaceutical preparation comprising micro-rna-143 derivative Disclosed is a benzene-pyridine derivative of microRNA-143, which is insusceptible to the degradation with a digestive enzyme (RNase). Also disclosed is use of the derivative for medical purposes. BP-microRNA-143, which has a higher activity than that of naturally occurring microRNA-143 and is insusceptible to degradation, is synthesized by matching at least one to three parts in a sense strand of a (noncomplementary) sequence having four mismatches in naturally occurring microRNA-143 (to the corresponding parts in a complementary sequence) and modifying the 3’-terminal of the resulting sequence with benzene-pyridine (BP).
US20120083459 Use of ganglioside to decrease propagation of malignant prostate cells Uses of exogenous ganglioside to inhibit the propagation of prostate cancer cells are provided. Gangliosides regulate many cellular processes including cell death. The present disclosure assesses the role of ganglioside in prostate cell growth. Malignant prostate (PC-3) and control (RWPE-1) cells can be cultured with or without ganglioside treatment. Cells can be assayed for differences in cell growth. Supplementation with ganglioside (GD3) can decrease growth of PC-3 cells by 30% compared to controls (p<0.01). Ganglioside can have therapeutic benefit in prostate cancer as demonstrated by decreased growth of malignant PC-3 cells.
WO2013147140A1 Nucleic acid molecule capable of inhibiting expression of periostin gene, method for inhibiting expression of periostin gene, and use of said nucleic acid molecule Provided is a novel molecule which can inhibit the expression of periostin gene. A nucleic acid molecule capable of inhibiting the expression of periostin gene is characterized by containing nucleotides that constitute at least one nucleotide sequence selected from the nucleotide sequences represented by SEQ ID NOs: 1 to 19 as a sequence capable of inhibiting the expression of periostin gene. The nucleic acid molecule capable of inhibiting the expression according to the present invention can inhibit the expression of periostin gene. Therefore, the nucleic acid molecule can be used for the treatment of eye diseases associated with the expression of periostin gene, specifically proliferative diabetic retinopathy, macular degeneration and the like.
WO2013056684A3 Thiazole derivative as dhodh inhibitor and use thereof A thiazole derivative, as represented in formula I, as a DHODH inhibitor and a use thereof. The compound of the present invention can be used for treating or preventing DHODH-mediated diseases, including, but not limited to, rheumatoid arthritis and autoimmune diseases such as anti-tumor, anti-organ transplant rejection, and anti-psoriasis.
WO2014084427A1 Composition comprising alginic acid for preventing or treating osteoarthritis The present invention relates to a composition comprising alginic acid, as an active ingredient, for treating or preventing osteoarthritis or osteoporosis. The composition for treating or preventing osteoarthritis or osteoporosis may be a pharmaceutical composition. Further, the present invention relates to a food composition comprising alginic acid, as an active ingredient, for alleviating or preventing osteoarthritis or osteoporosis. The composition of the present invention is identified as having an optimum condition for treating, preventing or alleviating osteoarthritis or osteoporosis in terms of the molecular weight of the alginic acid and mannuronate and guluronate. The composition of the present invention comprises alginic acid, as an active ingredient, which is harmless to humans, and therefore has no side effects and exhibits excellent effects in treating osteoarthritis or osteoporosis. Thus, the composition of the present invention can be effectively used in treating osteoarthritis or osteoporosis.
WO2012125071A1 1,3-diethylbenzimidazole salts - immunostimulating agents and pharmaceutical compositions on the basis thereof The invention relates to the field of immunology, in particular to agents for treating immunodeficiency disorders. The problem addressed by the invention is the production of novel preparations having a marked immunostimulating activity and being highly effective therapeutically, with a simultaneous decrease in undesirable side effects and a reduction in the cost of treatment. The problem is solved by substances which are active in the treatment of immunodeficiency disorders and are from the group of 1,3-diethylbenzimidazole salts of general formula: (I), where X- = an anion, and also by pharmaceutically acceptable compositions thereof.
WO2009075334A1 Uterine fibroid cell growth inhibitor, and prophylactic or therapeutic agent for uterine fibroid comprising the inhibitor The object aims to provide: a uterine fibroid cell growth inhibitor which is free from the risk of causing an adverse side effect including ovarian dysfunction and bone loss, and which can be administered over a long period; and a prophylactic or therapeutic agent for uterine fibroid. Disclosed are: a uterine fibroid cell growth inhibitor comprising an aldosterone receptor inhibitor as an active ingredient; and a prophylactic or therapeutic agent for uterine fibroid, which comprises the uterine fibroid cell growth inhibitor.
CN1739590A Dispersion tablet containing notoginseng total saponin and its prepn The present invention is dispersion tablet containing notoginseng total saponin and its preparation. The dispersion tablet contains notoginseng total saponin 25-34 weight portions, disintegrating agent 11-17 weight portions, stuffing 46-60 weight portions, and supplementary material including fine silicone gel 2-3 weight portions and magnesium stearate 0.2-0.3 weight portions. The dispersion tablet has excellent protecting effect on acute myocardial ischemia, and can lower the raised S-T section in cardiograph caused by myocardial ischemia, reduce the myocardial ischemia range caused by infarction and reduce serum lactic dehydrogenase content.
WO2012045196A1 Phosphoglycerate kinase inhibitors Disclosed are compounds of formula (I) or pharmaceutical acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined in the description. Disclosed are also the methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as phosphoglycerate kinase.
EP1165091B1 Pharmaceutical emulsions for retroviral protease inhibitors The present invention provides an emulsion formulation with high oral bioavailability containing lecithin as an emulsifier and solubilizing agent to achieve a high loading of the pyranone compound of formula (I).
EP1721601A1 Use of taurine for enhancing lipid synthesis in the epidermis Non-therapeutic cosmetic comprises taurine to stimulate the epidermal synthesis of lipid barrier. - ACTIVITY : Dermatological; Antiinflammatory. - MECHANISM OF ACTION : Epidermal synthesis of lipid barrier stimulator.
US20080070865 Inhibiting a taste modulating protein; used in pharmaceutical, food, and other products to inhibit certain taste functions and perceptions; side effects reduction The present invention is directed to the use of a compound having the formula wherein R1, R2, R3, m, n and p are defined herein. The compounds of the present invention are useful as inhibitors of certain taste perceptions and functions. The invention is also directed to compositions comprising a compound according to the above formula.
WO2008014661A1 Tetrahydroprotoberberine compounds, their manufacture, medicinal composition and uses. The present invention affords tetrahydroprotoberberine compounds listed as formula (I) and their pharmaceutically acceptable inorganic or organic salts, crystallized hydrates, solvates and medicinal compositions. In the formula (I), R1, R2, R3 and R4 represent H, lined or branched chain C1-4 alkyl, cyclopropyl, cyclopropyl methyl, methoxyl methyl, methoxycarbonylmethyl, aryl, benzyl, allyl, or substituted aryl or benzyl. R5 and R6 represent H, halogen, OH, SH, NO2, NH2, substituted or non-substituted lined or branched C1-4 alkyl. The configuration of C-14 is R, S or its racemate. The present invention also provides their preparation process and application in preparing medicine for treating neurological diseases, especially dopamine receptor related neurological diseases.
WO2008070902A1 Tgf-beta compositions for treating infertility This invention relates to pharmaceutical compositions of members of the TGF superfamily, and especially to compositions comprising members of the mammalian TGFβ superfamily, in which the composition comprises a substantially purified TGFβ, a zwitterion, and a pharmaceutically acceptable carrier. The zwitterion may be selected from the group consisting of an amino acid, a zwitterionic buffer compound, a zwitterionic detergent compound and an alkaloid. In some embodiments the invention relates to a composition comprising TGFβ, which is stable at pH 2.0 to 7.0 for at least 6 months at a temperature between 4° and 27°C.
CN101926759A Idebenone injection containing 2-hydroxylpropyl-beta-cyclodextrin and preparation method thereof The invention relates to an idebenone injection containing 2-hydroxylpropyl-beta-cyclodextrin and a preparation method thereof, which completely solve the water-solubility problem of idebenone, so that multiple injections can be prepared. The idebenone injection contains the 2-hydroxylpropyl-beta-cyclodextrin. The injection is realized in a way that the idebenone is dissolved in water by adding the 2-hydroxylpropyl-beta-cyclodextrin, wherein the proportion by weight of the idebenone to the 2-hydroxylpropyl-beta-cyclodextrin is 1:5-1:100. The injection comprises an injection, a freeze-dried powder injection, an aseptic powder injection, a menstrumm crystal powder injection, an idebenone glucose injection, an idebenone sodium chloride injection, an idebenone glucose and sodium chloride injection and the like. Through the invention, the idebenone injection can be convenient for clinical application.
US20100298329 Tolperisone and tolperisone-like drugs for the treatment of k-ras associated cancers The invention provides compositions and methods for treating cancer. Aspects of the invention relate to therapeutic compositions comprising tolperisone and related compounds. Aspects of the invention relate to methods and compositions for treating Ras-associated cancers.
CN1823754A Sodium bromophenolate eye drops and its preparation method An eye-drop of bromfenac sodium contains bromfenac sodium, sodium oxide as isotonic agent, water, pH regulator, metallic chelating agent, antioxidant, bacterial depressant and viscosity regulator. Its preparing process is also disclosed.
CN1559415A Application of ligo-xylose in preparing medicine for treating enteric function disturbance An application of oligoxylose in preparing the medicines in the form of powder, pill, capsule, tablet, etc for treating the intestinal function disorder (diarrhea, constipation, etc) is disclosed.
US7560548 antiinflammatory agent N-{[(2S)-4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}cyclopropane carboxamide; bronchitis, asthma, chronic obstructive pulmonary disease and rhinitis There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
CN103599112A Application of bufanolide diene compound in preparation of medicines for treating sepsis immune paralysis The invention relates to an application of a compound with a bufanolide diene structure mother nucleus in the preparation of medicines for treating sepsis immune paralysis. Cinobufagin derived from an amphibian toad is adopted. Experiments prove that the compound is capable of obviously reversing the survival rate of a mouse with the clinically simulated sepsis immune paralysis which is caused by the cecal ligature and puncture of a mouse and secondary salmonella hit and inhibiting the reduction of CD4+ and CD8+ cells of the spleen and the lymph gland of the mouse with the immune paralysis. On blood mononuclear cells of a clinical severe sepsis patient, the cinobufagin can reverse the reduction of the expression level of TH1 immune stimulating factors such as TNF (tumor necrosis factor)-alpha, GM-CSF (granulocyte-macrophage colony-stimulating factor) and IFN (interferon)-gamma which are caused by sepsis. On a normal human mononuclear cell endotoxin tolerance model which is caused by lipopolysaccharide (LPS), the cinobufagin can effectively reverse the reduction of expression capacity of mononuclear cell TNF alpha caused by secondary lipopolysaccharide hit. The compound has very high development value and application prospect.
US20120093947 Method of treating reactive airway disease A method of treating a reactive airway disease in a subject comprising administering at least one peroxidase inhibitor in association with administration of at least one β-agonist.
CN1615858A Compound bergenin dripping pill and its preparing method The compound bergenin dripping pill as one medicine for treating chronic bronchitis consists of medicine and supplementary material. The medicine includes bergenin and chlorphenamine maleate and accounts for 3-40 wt%; and the supplementary material is polyglycol and accounts for 60-97 wt%. The preparation process of the compound bergenin dripping pill includes mixing bergenin and chlorphenamine maleate, dropping in a dripping pill machine into liquid paraffin as cooling agent, sucking cooling agent with sucking cloth and selecting pill. The compound bergenin dripping pill has well dispersed bergenin medicine, effectively raised medicine dissolving degree and thus excellent cough relieving and phlegm eliminating effect in treating chronic bronchitis.
EP1383447A4 Stent-based delivery of statins to prevent restenosis Restenosis of arteries after angioplasty in inhibited by implanting in the treated artery a stent (100) having the struts (102) coated with a composition including a statin (106) having anti-restenotic activity. Such statins may also be incorporated in a collagen or polymer matrix (106) that forms a coating covering the struts (102) and interstices (104) of the stent (100).
EP1923058A1 Coated pharmaceutical composition comprising an S1P agonist or modulator The present invention provides an oral pharmaceutical composition comprising an S1P agonist and/or modulator having a coating.
US20120309811 P-glycoprotein-specific non-competitive peptide and peptidomimetic modulators The invention relates to a compound having structure (I), which acts as a non-competitive specific inhibitor of P-glycoprotein (P-gp for “Pleiotropic glycoprotein”) and which can be used as a drug, particularly for improving the effectiveness of chemotherapy treatments. The invention is therefore suitable for use in the medical field, particularly for the chemotherapeutic treatment of cancers or infections.
US20100197772 Tissue-Specific MicroRNAs and Compositions and Uses Thereof The invention provides for isolated nucleic acid sequences of newly discovered micro RNAs that have been identified to exist in normal Human B cells and/or in tumor-related Human B cells, using an integrated bioinformatics method and pipeline described herein.
CN103751100A Acyclovir emulsifiable paste The invention relates to an acyclovir emulsifiable paste, and belongs to the field of chemical medicinal preparations. The emulsifiable paste is prepared from the following raw materials with the total amount of 100 parts by weight: 2-5 parts of acyclovir, 4-10 parts of cetostearyl alcohol, 2-10 parts of monoglyceride stearate, 4-10 parts of white vaseline, 4-10 parts of glycerin, 0.5-2 parts of sodium dodecyl sulfate, 0.2-0.5 part of ethylparaben, 0.5-2 parts of dimethyl sulfoxide, 0.2-1.0 part of benzalkonium bromide solution with a concentration of 5 wt%, and the balance purified water. The acyclovir emulsifiable paste provided by the invention is good in quality stability, is capable of rapidly permeating skin and being reserved for a relatively long time, is convenient to use and good in patient tolerance, causes no adverse reactions, and is worth for clinic popularization and application.
CN103239429A Quick-dry type hand disinfection gel and preparation method thereof The invention relates to a disinfectant, and more particularly relates to quick-dry type hand disinfection gel and a preparation method thereof. The quick-dry type hand disinfection gel is prepared from the following raw materials in percentage by mass: 55%-60% of alcohol, 0.2%-0.5% of carbomer resin, 0.1%-0.3% of neutralizer, 3%-4% of butanediol, 3%-5% of PEG (polyethylene glycol), 0.01%-0.1% of vitamin E carboxylic ester, 0.5%-1% of antiseptic bactericide and the balance of deionized water. As the alcohol and DP 300 are compounded and a moisturizing skin protection component is added, the quick-dry type hand disinfection gel has a good synergistic effect, a durable sterilizing effect and a good skin protection function, and a disinfection effect is improved.
CN102614129B Enrofloxacin dry suspension The invention belongs to the technical field of antibiotic preparations for livestock and in particular discloses a dry suspension component containing enrofloxacin. The enrofloxacin dry suspension is prepared by the following steps: performing solid dispersion to the water-insoluble enrofloxacin; and mixing the enrofloxacin and auxiliary materials comprising suspending aid, wetting agent, diluent, sweetener, adsorbent and flow aid uniformly to prepare the enrofloxacin dry suspension which can be dispersed into water uniformly and is used for performing oral administration to livestock. The enrofloxacin dry suspension has the advantages of simple method, low cost, stable quality, good suspension effect in water, excellent palatability and the like. In addition, the enrofloxacin dry suspension has the advantages of convenience in use, long acting time of medicines, high bioavailability and the like.
US20110052588 Method of treating hepatocellular carcinoma Materials and methods for treating hepatocellular carcinoma in a mammal are disclosed. The methods comprise administering to a mammal a composition comprising a therapeutically effective amount of a zvegf3 antagonist in combination with a pharmaceutically acceptable delivery vehicle. Zvegf3 antagonists include anti-zvegf3 antibodies, mitogenically inactive receptor-binding zvegf3 variant polypeptides, and inhibitory polynucleotides.
US20070280929 Adjuvant in the form of a lipid-modified nucleic acid The present invention relates to an immune-stimulating adjuvant in the form of a lipid-modified nucleic acid, optionally in combination with further adjuvants. The invention relates further to a pharmaceutical composition and to a vaccine, each containing an immune-stimulating adjuvant according to the invention, at least one active ingredient and optionally a pharmaceutically acceptable carrier and/or further auxiliary substances and additives and/or further adjuvants. The present invention relates likewise to the use of the pharmaceutical composition according to the invention and of the vaccine according to the invention for the treatment of infectious diseases or cancer diseases. Likewise, the present invention includes the use of the immune-stimulating adjuvant according to the invention in the preparation of a pharmaceutical composition for the treatment of cancer diseases or infectious diseases.
EP2767280A1 Anemia of cancer improving / prophylactic agent Problem to be Solved An agent for ameliorating and/or preventing anemia, which is useful in the amelioration and/or prevention of cancerous anemia, and can improve the quality of life of a cancerous anemia patient without advancing cancer progression, is provided. Solution An agent for ameliorating and/or preventing cancerous anemia containing 5-aminolevulinic acid (ALA) or a derivative thereof, or a salt thereof is prepared. Preferably, a metal-containing compound such as sodium ferrous citrate is contained in these ALAs. As the above-mentioned ALAs, ALA; various esters such as ALA methylester, ALA ethylester, ALA propylester, ALA butylester, and ALA pentylester; and hydrochlorides, phosphates, and sulfates, and the like of these ALA esters can be preferably exemplified.
EP2227482A1 2',4'-substituted nucleosides as antiviral agents Embodiments of the invention are to compounds of formulae (A), (A'), methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2 ', 4 ' -substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
CN101112386A Smectite middle gut positioning releasing pellet and method for preparing the same The present invention is used for treating various acute and chronic diarrheas with the diseased parts at the colon and rectum, which can be packaged by small packages for oral administration and can be further made into other formulations for oral administration. The drug can not be released in the stomach and the small intestine after the oral administration of the drug, so as to ensure to transfer the drug to the colon quantitatively. The prevention has higher specificity to treat the colitis, which can improve the efficacy and has convenient administration.
WO2012002986A2 Decellularized and delipidized extracellular matrix and methods of use Compositions comprising decellularized and delipidized extracellular matrix derived from adipose or loose connective tissue, and therapeutic uses thereof. Methods for treating, repairing or regenerating defective, diseased, or damaged adipose or loose connective tissues or organs in a subject, preferably a human, and/or for tissue engineering, filing soft tissue defects, and cosmetic and reconstructive surgery, using a decellularized and delipidized adipose or loose connective tissue extracellular matrix of the invention are provided. Methods of preparing tissue culture surfaces and culturing cells with adsorbed decellularized and delipidized adipose or loose connective tissue extracellular matrix are also provided.
WO2013090840A1 2 -amino- pyrido [3, 2 -d] pyrimidine derivatives as hcv inhibitors A compound of Formula I : or a pharmaceutically acceptable salt thereof, wherein the substituents are described herein, methods of making the compounds as well as compounds of formula (I) for use in the treatment of HCV infection.
WO2009151069A1 Imidazothiazole derivative having 4,7-diazaspiro[2.5]octane ring structure Disclosed is a novel compound which can inhibit the interaction between Mdm2 (murine double minute 2) protein and p53 protein and has an anti-tumor activity. Specifically disclosed is an imidazothiazole derivative represented by formula (1) having various substituents, which can inhibit the interaction between Mdm2 protein and p53 protein and has an anti-tumor activity. [In formula (1), R1, R2, R3, R4, R5, Ar1 and Ar2 are as defined in the description.]
US8784862 Compounds and method for coating surfaces in a hemocompatible manner The invention concerns oligosaccharides and polysaccharides as well as the use of these oligosaccharides and/or polysaccharides, which contain the sugar unit N-acylglucosamine or N-acylgalactosamine for the production of hemocompatible surfaces as well as methods for the hemocompatible coating of surfaces with said oligosaccharides and/or polysaccharides, which imitate the common biosynthetic precursor substance of heparin, heparan sulphates and chitosan. The invention further describes methods for producing said oligosaccharides and/or polysaccharides and discloses various possibilities of using hemocompatibly coated surfaces. The invention relates particularly to the use of said oligosaccharides and/or polysaccharides on stents with at least one according to invention deposited hemocompatible coating, which contains an antiproliferative, antiinflammatory and/or antithrombotic active agent, methods for the preparation of said stents as well as the use of said stents for the prevention of restenosis.
WO2005004875A1 Medicinal composition for pulmonary administration An inhalant which contains as an active ingredient a compound having the following general formula (1) or a pharmacologically acceptable salt thereof. It is useful in, e.g., treatments for respiratory diseases. (Ar1 is optionally substituted phenyl; Ar2 is halophenyl; X is CH(OH), SO, or SO2; and n is 1 or 2.)
EP2418948A1 Antiadhesion agents Vitamin E succinate derivatives according to formula I: are described. These compounds can be included in pharmaceutical compositions, and can be used for the treatment of cancers such as metastatic cancer and as antiadhesive agents.
CN102089303A Nitrogenated heterocyclic compound Disclosed is a nitrogenated heterocyclic compound represented by general formula (1). The compound or a salt thereof exhibits a potent antagonistic activity on an EP1 receptor when administered to a human body or an animal. Therefore, the compound or a salt thereof is useful, for example, as an active ingredient for a pharmaceutical agent for preventing and/or treating overactive bladder. The compound or a salt thereof is also useful as an active ingredient for a pharmaceutical agent for preventing and/or treating a symptom such as frequent urination, urgency of urination or urinary incontinence. In the formula (1), G represents any one group of the following formulas (Q1)-(Q4); Cy represents the aromatic group or the like; X represents C and N; Y represents C, N, O and S; A1-2 represent the single bond or the like; R1-7, 9 represent H or the like; R1 and R4 as well as R4 and R5 form rings; and R8 represents the carboxyl group or the like.
US20060270624 Gapped 2' modified oligonucleotides Oligonucleotides and other macromolecules are provided that have increased nuclease resistance, substituent groups for increasing binding affinity to complementary strand, and sub-sequences of 2′-deoxy-erythro-pentofuranosyl nucleotides that activate RNase H enzyme. Such oligonucleotides and macromolecules are useful for diagnostics and other research purposes, for modulating protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to antisense therapeutics.
CN103709160A Alzheimer's disease prevention and treatment medicine and preparation method thereof The invention belongs to the technical field of medicines, and concretely relates to applications of an amaryllidaceae alkaloid compound in the acetylcholinesterase inhibition and the Alzheimer's disease prevention and treatment. The compound is Tortuosine, can be obtained by extracting from Lycoris sprengeri Comes ex Baker or other plants, separating and purifying, and can also be obtained through chemical synthesis. Experiments show that the Tortuosine has a strong inhibition effect on acetylcholinesterase, and the acetylcholinesterase inhibition activity of the Tortuosine is stronger than that of Galanthamine, so Tortuosine can be used for preparing acetylcholinesterase agents and Alzheimer's disease prevention and treatment medicines. The medicine contains an effective treatment amount of Tortuosine and a pharmaceutically acceptable carrier.
CN101732342A Oral rehydration salt effervescent tablet and application thereof The invention discloses an oral rehydration salt effervescent tablet which mainly contains sodium chloride, postassium chloride, anhydrous dextrose, citric acid, sodium bicarbonate and/or sodium carbonate and water-soluble lubricant. The invention also discloses the application of the oral rehydration salt effervescent tablet. The oral rehydration salt effervescent tablet is convenient to carry and use. The dosages of an acid source and an alkali source in the oral rehydration salt effervescent tablet can reflect the dosage of sodium citrate needed by the prescription for producing oral rehydration salt (ORSII), thereby reducing the addition of the raw material sodium citrate and lowering the production cost effectively.
US20050119350 Treatment of effect of chemicals with their ultradilute stereoisomers A method of treating an effect of a chemical agent, which agent is characterized by one or more chiral centres, by administering a dilution or an ultra-high dilution or potentised preparation of a stereoisomer of said chemical agent.
CN1981773A Medicinal preparation for treating immune related diseases A medicine for treating the immune associated diseases including immune associated hematopathy, such as myeloproliferative syndrome, simple anerythroregenerative anemia, aplastic anemia, primary thrombopenic purpura, etc, contains sodium bicarbonate and ethiophosphate.
US20080153811 methods for treating, managing and preventing cognitive impairment associated with various diseases and disorders, age-associated memory impairment, and dementia. This invention relates to methods for treating, managing and preventing cognitive impairment associated with various diseases and disorders, age-associated memory impairment, and dementia.
CN101574501B Sanchi and combined spicebush root paste used for preventing and treating cervical spondylosis The invention relates to the field of medicament formulas, in particular to sanchi and combined spicebush root paste used for preventing and treating cervical spondylosis, which is prepared from raw materials of sanchi, combined spicebush root, nutgrass galingale rhizome, gentiana macrophylla, szechuan lovage rhizome, Yanhusuo, turmeric, eucommia bark, dahurian angelica root, borneol, nux vomica,dragon blood, red paeony root, garden balsam stem and suberect spatholobus stem; the raw materials are dried, ground into fine powder, and sieved by a 80-mesh sieve to obtain fine medicinal powder; and the fine medicinal powder is put into a proper amount of white spirit, stirred evenly and decocted by low fire into the paste. The sanchi and combined spicebush root paste is characterized in that:the raw materials by weight percentage are 11 to 14 percent of the sanchi, 9 to 11 percent of the combined spicebush root, 7 to 9 percent of the nutgrass galingale rhizome, 6 to 8 percent of the gentiana macrophylla, 5 to 7 percent of the szechuan lovage rhizome, 6 to 8 percent of the Yanhusuo, 3 to 5 percent of the borneol, 4 to 6 percent of the eucommia bark, 5 to 7 percent of the dahurian angelica root, 5 to 7 percent of the turmeric, 4 to 6 percent of the nux vomica, 3 to 5 percent of the dragon blood, 4 to 6 percent of the red paeony root, 7 to 9 percent of the garden balsam stem and 6 to8 percent of the suberect spatholobus stem. The sanchi and combined spicebush root paste has low cost of raw materials, high curative effect of preventing and treating the cervical spondylosis, no toxic and side effects.
CN103655580A Pharmaceutical composition containing valsartan, amlodipine besylate and hydrochlorothiazide and preparation method thereof The invention belongs to the field of medical technology and particularly relates to a pharmaceutical composition containing valsartan, amlodipine besylate and hydrochlorothiazide and a preparation method thereof. The pharmaceutical composition is composed of the following components in parts by weight: 160 parts of valsartan, 5 parts of amlodipine besylate (based on the weight of amlodipine), 12.5 parts of hydrochlorothiazide, 120 parts of microcrystalline cellulose, 16 parts of croscarmellose sodium, 3 parts of magnesium stearate, 12 parts of opadry and a proper amount of purified water; the pharmaceutical composition is prepared by a wet granulating and tabletting process. The pharmaceutical composition disclosed by the invention has the advantages of good content uniformity, stabile property and simple preparation process.
CN101249067A Anticancer sustained-release injection containing tumour medicament-resistant reverse agent and cell toxicity medicament An anticancer sustained-release injection is provided, which contains tumor multidrug resistance reversal agent and cytotoxic drugs. The anticancer sustained-release injection comprises sustained-release microspheres and solvents, wherein the sustained-release microspheres contain anticancer active components and sustained-release adjuvant, and the solvents are special solvents containing a suspending agent. The anticancer active components comprise a tumor multidrug resistance reversal agent selected from nelarabine, zarnestra, ropinirole and valspodar and/or a cytotoxic drug selected from cyclophosphamide, carmustine, nimustine, camptothecin, paclitaxel, cisplatin, carboplatin, vincristine, buthionine sulfoximine, O6-benzyladenine and O4-benzyl folic acid. The sustained-release adjuvant is selected from polifeprosan, di-fatty acid-decanedioic acid copolymer, polylactic acid and EVAc. The suspending agent has a viscocity of 100-3000 cp (25-30 DEG C) and is preferably sodium carboxymethylcellulose. The sustained-release microspheres can also be formulated as sustained-release implants or gel injections for injection or implantation in tumors or around tumors, to inhibit tumor cells and selectively enhance the therapeutic effect of nonoperative treatment such as chemotherapy.
WO2012099871A1 Modulation of lrch4 activity and therapeutic application thereof Disclosed herein are methods for altering cellular functions and processes by modulating the activity of Lrch4. Corresponding compositions that may be used in carrying out the described methods are also disclosed as are related methods of treatment for relevant diseases and physiological states.
CA2207779C Carcinoma treatment For the treatment of carcinomas in epithelial cells and for the prevention of epithelial cell proliferation, use is made of a CD40 receptor binder. The CD40 may be used in conjunction with at least one antineoplastic agent and/or CD40 inducer.
DE10360151A1 New 3-oxo-1-propenyl azo compounds useful as 5-HT receptor antagonists e.g. for treating psychoses, neurological disorders, amyotrophic lateral sclerosis and eating disorders 3-Oxo-1-propenyl azo compounds (I) and their salts, solvates and isomers are new. - 3-Oxo-1-propenyl azo compounds of formula (I) and their salts, solvates, diastereoisomers, enantiomers, racemates and mixtures of their enantiomers are new: - R1, R2 = aryl or heteroaryl optionally substituted with Q, A, halo, 3-7C cycloalkyl, CF3, NO2, CN, C(NH)NOH, OCF3, OA, NHA, NAA or NH2; - Q = aryl or heteroaryl optionally substituted with Ar, A, halo, 3-7C cycloalkyl, CF3, NO2, CN, C(NH)NOH, OCF3, OA, NHA, NAA or NH2; - R3 = H or an organic group, especially (CH2)nCO2R5, (CH2)nCOHet, (CH2)nOR5, (CH2)nHet, (CH2)nN(R5)2, CH=N-OA, CH2CH=N-OA, (CH2)nNHOA, (CH2)n(R5)Het, (CH2)nCH=N-Het, (CH2)nOCOR5, (CH2)nN(R5)CH2CH2OR5, (CH2)nN(R5)CH2CH2OCF3, (CH2)nN(R5)C(R5)COOR5, (CH2)nN(R5)CH2COHet, (CH2)nN(R5)CH2Het, (CH2)nN(R5)CH2CH2Het, (CH2)nN(R5)CH2CH2N(R5)CH2CO OR5, (CH2)nN(R5)CH2CH2N(R5)2, CH=CHCOOR5, CH=CHCH2NR5Het, CH=CHCH2N(R5)2, CH=CHCH2OR5 or (CH2)nN(R5)Ar; - A = 1-10C alkyl or alkoxy or 2-10C alkenyl or alkenyloxyalkyl; - Het = a saturated, unsaturated or aromatic, mono or bicyclic heterocyclic group, or linear or branched organic group containing one or more heteroatoms (all optionally substituted with one or more A and/or halo); - Ar = phenyl optionally substituted by one or more A and/or halo, OR5, OOCR5, COOR5, CON(R5)2, CN, NO2, NH2, NHCOR5, CF3 or SO2CH3; - R5 = H or A; - halo = F, Cl, Br or I; and - provided that when X = CH, then R2 and R4 are not both H - An INDEPENDENT CLAIM is also included for the preparation of (I). - ACTIVITY - Neuroleptic; Neuroprotective; Eating-Disorders-Gen.; Tranquilizer; CNS-Gen.; Antiinflammatory; Cerebroprotective; Antiparkinsonian; Antidepressant; Hypotensive; Antimigraine; Nootropic; Antiaddictive; Antialcoholic; Antismoking; Antianginal; Vasotropic; Analgesic; Anticoagulant; Thrombolytic; Gastrointestinal-Gen.; Cardiovascular-Gen.; Ophthalmological; Gynecological. - MECHANISM OF ACTION - 5-HT receptor antagonist.
EP2011507A2 Pharmaceutical composition of nateglinide and another antidiabetic agent The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide (l) or repaglinide and at least one other antidiabetic compound selected from the group consisting of thiazolidinedione derivatives (glitazones), sulfonyl urea derivatives and metformin for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of diseases, especially metabolic disorders and in particular type 2 diabetes and diseases and conditions associated with diabetes; to a composition, respectively, which comprises nateglinide and a pharmaceutically acceptable carrier and to a process of making such composition; the use of such combination or composition for the preparation of a medicament for the prevention, delay of progression or treatment of metabolic disorders; a method of prevention, delay of progression or treatment of diseases in warm-blooded animals; the use of such combination or composition for the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body weight; and to a method of improving the bodily appearance of a warm-blooded animal.
CN101829243A External quick-acting cream for psoriasis and acne and production process The invention discloses external quick-acting cream for psoriasis and acne and a production process. Based on the total weight of 100 percent, the cream contains the following raw materials in percentage by weight: 4 to 5 percent of peach branch extract, 4 to 5 percent of clerodendrum bungei extract, 8 to 10 percent of perilla leaf extract, 8 to 10 percent of potassium sorbate, 45 to 50 percent of deionized water and 25 to 30 percent of kaolin, wherein the peach branch extract is water-soluble dry powder, contains 1 to 1.6 percent of natural plant antibiotic of alkaloid property, and also contains amyrin, naringenin, persicoside, persicogenin and purpurein; the clerodendrum bungei extract is water-soluble dry powder, contains colorless wax, and also contains clerodendron trichotomum alesin, clerodendron trichotomum A and B, acacetin-7 diglucuronide and meso-inositol; and the perilla leaf extract is dry powder, and contains 12 organic active ingredients such as alpha-bergamot oil alkene, laurolene, beta-sitosterol and the like. The external quick-acting cream has quick effects of resisting bacteria, tumor and psoriasis, repairing various kinds of psoriasis and acne and eliminating focuses.
US20110015151 Combination of viscoelastics for use during surgery An improved viscoelastic composition useful in the performance of ophthalmic surgical procedures and especially cataract procedures is disclosed. The embodiments of the composition comprise combinations of sodium hyaluronate and chondroitin sulfate and exhibit an improved rheological profile.
EP1492595A1 Therapy for psychoses combining an atypical antipsychotic and an mglu2/3 receptor agonist The present invention provides for a pharmaceutical composition and methods for treating psychosis comprising the combination or a first component which is an atypical antipsychotic with a second component which is a mGlu2/3 receptor agonist. The present invention also provides for a pharmaceutical composition and method of treating a psychiatric disorder comprising the combination of a first component which is an atypical antipsychotic with a second component which is a compound which allosterically enhances receptor activity for mGlu2 and/or mGlu3.
CN103494785A Montelukast sodium chewable tablet and preparation method thereof The invention belongs to the technical field of medicines and particularly relates to a montelukast sodium chewable tablet and a preparation method thereof. The montelukast sodium chewable tablet provided by the invention is composed of montelukast sodium, a diluting agent, a lubricating agent, a binding agent, a disintegrating agent, a coloring agent, a sweetening agent and a corrigent. A preparation process of the montelukast sodium chewable tablet adopts absolute ethyl alcohol as a solvent to prepare the binding agent and then the binding agent is mixed with powder of other raw materials and auxiliary materials to carry out wet-method granulation. After being dried, wet grains are mixed with the corrigent and the lubricating agent and then a mixture is tabletted. According to the montelukast sodium chewable tablet prepared by using the process method provided by the invention, the color and the luster of the appearance of the tablet are uniform and bright, the stability is good, the disintegrating speed is high and the bioavailability is high.
US20090099168 HIV Integrase inhibitors Pyridopyrazine- and pyrimidopyrazine-dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula I: wherein G, Q, bond a, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
CN103664871A Isoquinoline derivative salt The invention relates to 4-(2-pyrryl)-1-isoquinoline-3-methyl formate as well as fumarate of derivative thereof or pharmaceutically acceptable solvant and application in preparing medicaments for treating the cancer.
US8114603 collecting a blood sample from the subject; andmeasuring the levels of Triggering Receptor Expressed on Myeloid cells (TREM-1) splice variant protein in sample, a decrease in the levels of TREM-1 splice variant indicates an inflammatory response The present invention relates to a soluble receptor variant of TREM-1. More particularly, present invention relates to methods of modulating an immune response by administering variants of TREM-1.
CN103182053A Medicament for treating whooping cough, and preparation method thereof The invention discloses a medicament for treating whooping cough, and a preparation method thereof. The medicament is mainly prepared by aristolochia fruit, peppergrass, perilla seed, bryozoatum, tatarian aster root, bitter orange, hogfennel root and dark plum according to a certain weight proportion. The medicament has the functions of regulating Qi, strengthening spleen, expelling phlegm, arresting coughing, nourishing yin and clearing away the lung heat, and is quick in action, good in curative effect and high in cure rate.
CN101318020B Anti-anxiety or/and dumps medicament composition and uses thereof The invention provides a use of Alpha2 adrenergic receptor agonist with efficient dosage in preparing a medicament which is given together with 5-HT 1A receptor agonist with efficient dosage and is used for anti-anxiety or/and anti-depression. The invention also provides an anti-anxiety or/and anti-depression drug combination, which is a medicament prepared by the raw materials of Alpha2 adrenergic receptor agonist with efficient dosage and 5-HT 1A receptor agonist with efficient dosage, wherein, the weight proportion of Alpha2 adrenergic receptor agonist and 5-HT 1A receptor agonist is: 0.2-125 shares of Alpha2 adrenergic receptor agonist and 5-16 shares of 5-HT 1A receptor agonist. In the invention, the two drugs are used together, especially the optional tizanidine hydrochloride and tandospirone citrate are used together so as to have the function of increasing effect, and the side effect is low, effect taking is stable, thus solving the problem which can not be overcome presently and providing a new choice for clinic.
EP1828178A1 Process for preparation of high-purity meloxicam and meloxicam potassium salt The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium sait monohydrate is produced. Said sait is subsequently treated with minerai or organic acid to yield high-purity meloxicam.
WO2014039908A1 Methods and compositions for regenerating hair cells and/or supporting cells Provided are methods and compositions for inducing cells of the inner ear (for example, cochlear and utricular hair cells) to reenter to cell cycle and to proliferate. More particularly, the invention relates to the use of agents that increase c-myc activity and/or Notch activity for inducing cell cycle reentry and proliferation of cochlear or utricular hair cells and/or cochlear or utricular supporting cells. The methods and compositions can be used to promote the proliferation of hair cells and/or supporting cells to treat a subject at risk of, or affected with, hearing loss or a subject at risk of, or affected with vestibular dysfunction.
US20100266491 System for targeted delivery of therapeutic agents The present invention provides a drug delivery system for targeted delivery of therapeutic agent-containing particles to tissues, cells, and intracellular compartments. The invention provides targeted particles comprising a particle, one or more targeting moieties, and one or more therapeutic agents to be delivered and pharmaceutical compositions comprising inventive targeted particles. The present invention provides methods of designing, manufacturing, and using inventive targeted particles and pharmaceutical compositions thereof.
CN103690552A Pharmaceutical composition and application thereof to preparing pharmaceutical preparation for treating hepatitis B The invention relates to a pharmaceutical composition and application thereof to preparing a pharmaceutical preparation for treating hepatitis B. Compared with single drugs, found from researches, the pharmaceutical composition disclosed by the invention has obvious enhanced inhibiting effect to hepatitis B virus (HBV) and can be used as the therapeutic drug of hepatitis-B patients.
CN102225046A Transdermal drug delivery formulation The present invention provides a transdermal formulation for the delivery of at least one active agent. The formulation includes (i) a first compound comprising an organic sulfoxide, and (ii) a second compound selected from the group consisting of a fatty acid ester, a fatty acid, an azone-related compound and mixtures thereof.
US20080064709 Methods and compositions for the treatment of vascular depression Methods and compositions are provided for treating vascular depression. The methods involve administering to a subject in need thereof a xanthine derivative in a therapeutically effective amount to treat vascular depression, particularly the xanthine derivatives pentoxifylline or propentofylline. The methods may further include administration of an additional therapeutic agent in combination with the xanthine derivative selected from the group consisting of a selective serotonin reuptake inhibitor (SSRI), a serotonin-norepinephrine reuptake inhibitor (SNRI), and a drug used in the treatment of cerebrovascular disease. Compositions of the invention include pharmaceutical compositions and kits for treating vascular depression in a subject in need thereof that include therapeutically effective amounts of a xanthine derivative and an additional therapeutic agent selected from the group consisting of an SSRI, an SNRI, and a drug used in the treatment of cerebrovascular disease.
US20090227641 Cycloalkylamino acid derivatives The invention relates to compounds of formula I and to pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof. This invention also relates to a method of using such compounds in the treatment of hyperproliferative diseases and autoimmune diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
US20080221150 Inhibit neurodegeneration caused by lysosomal and/or mitochondrial dysfunction; bafilomycin A1, bafilomycin B1 and concanamycin The present disclosure describes the use of macrolide antibiotics to prevent neurodegeneration and to treat or prevent disease and conditions which involve neurodegeneration. While not being limited to a specific mechanism of action, in one embodiment, the macrolide antibiotics inhibit neurodegeneration caused by lysosomal and/or mitochondrial dysfunction. The present disclosure contemplates the use of any macrolide antibiotic and pharmaceutically acceptable derivatives thereof. In a specific embodiment, the macrolide antibiotics include bafilomycin A1, bafilomycin B1 and concanamycin.
US20100317684 Amide and Carbamate Derivatives of N-{2-[4-Amino-2- (Ethoxymethyl)-1H-Imidazo[4,5-c] Quinolin-1-Yl]-1,1-Dimethylethyl} Methanesulfonamide and Methods Amide and carbamate derivatives N-{2-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-1,1-dimethylethyl}methanesulfonamide, pharmaceutical compositions containing these compounds, methods of making the compounds, and methods of use of these compounds in modulating the immune system, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
WO2011136561A3 Composition for the treatment of vitiligo, containing serotonin as an active ingredient The present invention relates to a composition for the prevention or treatment of vitiligo, which contains serotonin or a derivative thereof as an active ingredient, and to a method for screening pigmentation inhibitors. More particularly, serotonin facilitates an increase in melanin biosynthesis and the migration of melanin cells by serotonin receptor 2A, and therefore can be effectively used in the treatment of vitiligo. According to the present invention, a material which increases or inhibits melanin biosynthesis in a serotonin receptor 2A-specific manner can be developed.
CN101502533A Novel hydrocarbonate dialysis powder The invention relates to a novel bicarbonate dialysis powder, belonging to biomedical materials and comprising powder A and powder B, wherein, the powder A comprises the following components: 950 to 1063 parts of sodium chloride, 19.6 to 45.7 parts of potassium chloride, 17.8 to 26.7 parts of magnesium chloride, 32.2 to 45 parts of calcium chloride and 100 to 198 parts of solid acetic complex; and the powder B comprises the following component: 504 to 655 parts of sodium bicarbonate, wherein, the solid acetic complex is prepared from glacial acetic acid by adopting the one-step synthesis method; and the components in the powder A are mixed by the formula thereof on the basis of the equivalent-increasing method. The invention has the advantages that the solubility of the product is high, and the problem that the dialysis powder tends to be 'hardened' after the chlorides and the glacial acetic acid in the powder A are mixed during the process of storage is resolved; and the invention improves the stability of the conductivity, maintains the stability of the pH value, improves the storage performance of the product and prevents the heavy acid taste from irritating medical personnel during the preparation process of dialysate.
CN101143167A Medicine for treating cancer and preparing method thereof The invention relates to a drug for remedying the cancer and especially indicates a cancer-washing cure drug of Hunan He pharmacy for remedying the cancer. The invention has good curative effect within the following weight range of 7 to 15 portions of duchesneas, 7 to 15 portions of sun euphorbia, 7 to 15 portions of prepared pinellia tubers, 7 to 15 portions of alums, 5 to 15 portions of rhubarbs and 450 to 550 grams of liquor. The preparation method of active components of the drug of the invention is as follows that the raw materials of the duchesnea, the sun euphorbia, the prepared pinellia tuber, the alum and the rhubarb are washed cleanly for using; the raw materials are dipped in the liquor of high quality in an urn; the drug can be taken out for using after one month.
WO2009142589A1 Combination of (a) glucocorticoid receptor modulator and (b) a muscarinic antagonist The present invention relates to a combination of (a) a glucocorticoid receptor modulator and (b) a muscarinic antagonist. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treatment of airway diseases, such as chronic obstructive pulmonary disease (COPD) and asthma in mammals by administrating said combination. The invention also relates to a kit comprising the combination and use of said kit in treatment of airway diseases.
CN103520136A Montelukast sodium pulse capsule and preparation method thereof The invention discloses a montelukast sodium pulse capsule capable of releasing drugs in specific time. The montelukast sodium pulse capsule disclosed by the invention consists of a quick-release part and a release regulation part, wherein the quick-release part consists of quick-release powder or quick-release particles, and the powder or particles of the quick-release part is/are made from hydrophilic accessories; the release regulation part consists of release regulation particles, and the release regulation particles are covered with an exterior coating consisting of one or more pH dependent polymers. Compared with a common preparation, by adopting the pulse release capsule disclosed by the invention, the blood concentration reaches the peak when asthma easily attacks before dawn, the aim of hour treatment can be achieved, and the effectiveness and safety of drugs for asthma patients are improved.
US6919359 Azabicyclic-substituted-heteroaryl compounds for the treatment of disease The invention provides compounds of Formula I: Azabicyclo-N(R1)—C(═X)—W Formula I These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which α7 is known to be involved.
CN101605545A Skin adhesive preparation comprising stabilized donepezil To provide a donepezil-containing skin adhesive preparation in which the production of a donepezil analogue in an adhesive layer is prevented. [MEANS FOR SOLVING PROBLEMS] One or more stabilizers are added to a donepezil-containing adhesive layer provided on at least one surface of a substrate, wherein the one or more stabilizers are selected from the group consisting of ascorbic acid or a metal salt or ester thereof, isoascorbic acid or a metal salt thereof, ethylenediaminetetraacetic acid or a metal salt thereof, cysteine, acetylcysteine, 2-mercaptobenzimidazole, 3-(2)-t-butyl-4-hydroxyanisole, 2,6-di-t-butyl-4-methylphenol, pentaerythritol tetrakis[3-(3',5'-di-t-butyl-4'-hydroxyphenyl)propionate], 3-mercapto-1,2-propanediol, tocopherol acetate, rutin, quercetin, hydroquinone, a hydroxymethanesulfinate metal salt, a metabisulfite metal salt, a sulfite metal salt and a thiosulfate metal salt.
US20110003804 Oxazolidinones For the Treatment and/or Prophylaxis of Heart Failure The present invention relates to the use of selective inhibitors of coagulation factor Xa, in particular of oxazolidinones of the formula (I), for the treatment and/or prophylaxis of heart failure and/or disorders related to heart failure as well as their use for the preparation of pharmaceutical drugs for the treatment and/or prophylaxis of heart failure and/or disorders related to heart failure.
CN103690508A Tablet composition containing pitavastatin calcium and preparation method of tablet The invention discloses a tablet composition containing pitavastatin calcium and a preparation method of the tablet composition. The tablet composition contains main medicine-pitavastatin calcium, porous filler, a disintegrating agent, a lubricating agent and opadry film premix. A direct powder compression method is adopted; the stability of a product is remarkably improved.
WO2007037423A1 Antidiabetic agent A novel antidiabetic agent which contains carthamidine (1) and/or isocarthamidine (2) as an active ingredient.
US20110217388 Devices and methods for the regeneration of bony defects This invention relates to methods for producing a composite bone graft material that can regenerate bony defects in the body. The invention further relates to methods that allow for the production of bioactive glass particles used in the composite that have been surface treated to allow for the production of a highly porous composite that can hold significant amounts of body fluid or other molecules that will aid in the regenerative process. The method of surface treatment allows for the manufacture of a suitable implantable composite while retaining the unique osteostimulative properties that are associated with bioactive glass particles.
WO2008005194A3 Method for the eradication of pathogens comprising generating molecular iodine in situ A method for killing or substantially eradicating a pathogen in the upper respiratory tract of a mammal is disclosed. The method comprises generating molecular iodine (12) in situ using an oxidant-reductant reaction with a minimum concentration of at least about 25 ppm of I2 and I2 comprises at least 40% of the total iodine atoms. A method for inhibiting superantigens using molecular iodine is also disclosed.
US20130028869 Feed supplement comprising oligosaccharides and medium chain fatty acids The present invention relates to a feed supplement and a feed containing this feed supplement, comprising 1) a homotrimer, heterotrimer, homotetramer and/or heterotetramer of a carbohydrate component selected from the group consisting of a pentose saccharide, a hexose saccharide, glucuronic and galacturonic acid, and 2) a medium-chain fatty acid (MCFA), selected from the group consisting of caproic acid (C6), caprylic (C8), capric (C10) and lauric acid (C12). The invention also refers to the use of the feed supplement or feed in order to improve the efficiency of animal production, such as weight gain, feed conversion, nutritive value, health and wellbeing through the selective elimination of enteropathogens.
US7101574 Pharmaceutical composition containing fenofibrate and the preparation method The invention concerns a pharmaceutical composition containing micronized fenofibrate, a surfactant and a binding cellulose derivative, as solubilizing adjuvant, preferably hydroxypropylmethylcellulose. The cellulose derivative represents less than 20 wt. % of the composition. The association of micronized fenofibrate with a binding cellulose derivative, as solubilizing adjuvant and a surfactant enables enhanced bioavailability of the active principle. The invention also concerns a method for preparing said composition without using any organic solvent.
CA2844765A1 Polymorph of rifaximin and process for the preparation thereof The present invention relates to a new polymorph of Rifaximin, designated ?, and to a process for the preparation thereof. Under certain aspects, the invention also relates to pharmaceutical compositions comprising an effective amount of the polymorphic form ? of Rifaximin and a pharmaceutically acceptable carrier and its uses in the treatment of gastrointestinal conditions.
WO2007059620A1 Method for administering formoterol using a nebulizer The present invention provides a method of administering formoterol, for example as a fumarate dihydrate, using a nebulizer device for the treatment of bronchoconstriction, such as that caused by asthma and chronic obstructive pulmonary disease. The method of this invention is particularly useful in pediatric, geriatric, handicapped and acutely ill individuals who have been denied the benefits of this medication due to the standard use of dry powder inhalers. The present invention addresses the difficulty of making available a viable commercial nebulizer solution for these individuals who cannot optimally use powder inhaler devices, which are the only presently available delivery systems for this medication.
WO2011083637A1 Therapeutic agent for hepatic disorder Provided is a method for controlling the interaction between Keap1 and p62 which control the formation of an ubiquitin-positive inclusion body.
CA2672585A1 Composition containing agaricus blazei murill Disclosed is a composition comprising a fruit body of Agaricus blazei murill or an extract from the fruit body and an amino acid involved in the ornithine cycle or a salt thereof, wherein the pharmacological activities of the fruit body of Agaricus blazei murill or the extract from the fruit body and the amino acid involved in the ornithine cycle or the salt thereof are increased synergistically. Specifically disclosed is a composition comprising 1 part by weight of a fruit body of Agaricus blazei murill or an extract from the fruit body and 10 to 100 parts by weight of an amino acid involved in the ornithine cycle or a salt thereof.
US8088828 Treating benign prostate hyperplasia with SARMS This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-α reductase enzyme type 1 and/or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-α reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-α reductase inhibitory amount of a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, as described herein.
CN102949459A Medicinal composition for reducing blood sugar and capsule preparation method of the medicinal composition The invention discloses a medicinal composition for reducing blood sugar and a capsule preparation method of the medicinal composition. The medicinal composition contains the following components in parts by weight: 20 parts of bitter gourd, 15 parts of radix astragali, 20 parts of fenugreek, 5 parts of folium mori, 20 parts of propolis and 20 parts of picolinic acid. According to the invention, the medicinal composition is expected to reach an effect of reducing blood sugar, and is prepared by the bitter gourd, the radix astragali, the fenugreek, the folium mori, the propolis and the picolinic acid as the main raw materials based on a scientific and reasonable production technology. The medicinal composition is definite in function, controllable in quality and safe to take. According to the invention, the preparation method of the capsule preparation of the medicinal composition is simple, and the preparation of the capsule preparation can be finished by conventional equipment.
CN101138551A Preparation method of lung targeting emodin polylactic acid microsphere and application in anti-mouse pulmonary fibrosis The present invention relates to the preparation method of a lung-targeted emodin poly lactic acid micro sphere and the application in inhabiting the pulmonary fibrosis of the mice. The present invention is characterized in the following method. 0.5 to 1.5 portion of emodin and 2.5 portions to 3.5 portions of polydactyl acid are precisely measured before mixing in mixed solvent, which comprises dichloromethane and ace according to a ratio of from 2.5 till 3.5 to from 0.5 till 1.5. The mixed solvent is slowly added into the dispersed medium glycerol with the mixing speed of 400 to 600 rotations per minute. The mixed suspension system is formed after 8 minutes to 12 minutes mixing. The mixed suspension system is added into the dispersed medium of 0.4 percentages to 0.6 percentage of gelatin after uniform dispersion. The liquid is mixed at the speed of 400 to 600 rotations per minute for 8 minutes to 12 minutes before micro sphere solidification. The centrifugation is conducted at 2700 -3300 rotation per minute for 13 minutes to 17 minutes after standing for 25 minutes to 35 minutes. The micro spheres are collected before sucking filtration with the water system filter membrane, followed by washing with the distilled water for 3 times to 5 times. The powder-typed emodin poly lactic acid micro sphere is obtained after drying by the phosphori pentoxidum vacuum drying apparatus. The distribution of the emodin poly lactic acid micro sphere has lung targeting property with obvious slow-releasing property in vitro. The application of the medicine in pulmonary fibrosis of the mice proves that the medicine has good therapy effect in the pulmonary fibrosis of the mice. The present invention displays the application prospect in treatment of the pulmonary fibrosis.
CN101313901A Medicine uses of herpetone The invention relates to a medicinal application of a compound, namely herpetrione. The invention discloses the application of the herpetrione in preparation of medicines for liver damage resistance, liver cancer resistance and so on for the first time, in particular relating to the application of the herpetrione in preparation of medicines for treating the liver damage caused by chemical substances. The invention also provides a medicine which takes the herpetrione as an active ingredient, treats the liver damage and resists the liver cancer. The medicine provides a novel choice for clinic therapy of the liver damage and the liver cancer.
US7144909 Phenoxy substituted benzocondensed heteroaryl derivatives as thyroid receptor ligands This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subcllinical hyperthyrodism and liver diseases.
US20110275645 Small Molecules for Inhibition of Protein Kinases The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.
WO2005000205A2 Methods and compositions for modulating serum cortisol levels The present invention relates to cortisol-modulating compounds, inlcluding but not limited to benzamide and benzoic acid derivatives such as procaine and procaine derivatives, utilized in compositions and methods for treating cortisol-mediated disorders, including but not limited to age-related depression, hypertension, Alzheimer's disease, and acquired immunodeficiency syndrome.
CN102793833A Onion, celery, leek and chromium thrombolytic tablets The invention discloses onion, celery, leek and chromium thrombolytic tablets, and belongs to a latest product special for treating hypertension and thrombolysis at present. The thrombolytic tablets are prepared from daily vegetables, concentrated juice and chromium serving as a trace element. The thrombolytic tablets are novel and unique in formula, easy and feasible to take and good in effect, and can be eaten and drunk to fulfill the purpose of reducing blood pressure.
WO2009095634A1 Amorphous forms of retapamulin The present invention is directed to amorphous forms of retapamulin, methods of making the amorphous forms, pharmaceutical formulations containing the same, therapeutic uses thereof and methods of treatment employing the same.
CN101057677B Xinxi nutrient supplement The invention discloses a nutrient enhancer which can be prepared into dosage forms of tablets, capsules, powders and oral liquids, and comprises constituents of zinc element and vitamin C, the minimum dosage of each form include zinc element 2. 5-25mg and vitamin C 25-500mg.
CN101862316A Application of vanillic acid in prevention and treatment of radiation injury The invention relates to novel application of vanillic acid in the prevention and the treatment of radiation injury. Experiments prove that the vanillic acid has no toxicity to V79 cells within a concentration range of smaller than 100mug/ml; the vanillic acid has a dose-dependent suppression function to the devitalization of the V79 cells caused by 60Co gamma rays at 0.2 to 5mug/ml; and the survival rate of a BALB/c mouse with the 6Gy irradiation of the 60Co gamma rays can be enhanced in a dose-dependent way by supplying 100 or 200mg/kg of vanillic acid in a preventive way, which shows that the vanillic acid can be used for preventing and treating the radiation injury.
EP2759294A1 Percutaneously absorbable preparation containing fentanyl and a homologue thereof Disclosed is a transdermal preparation, comprising sequentially-stacked layers of a backing layer, a barrier layer, a drug adhesive layer and a release layer, wherein the drug adhesive layer contains a drug selected from the group consisting of fentanyl, an analogue thereof and a pharmaceutically-acceptable salt thereof, a skin permeation enhancer of the drug, and a polyacrylate adhesive, which shows a high skin permeation with a low drug dosage, equivalent to one with high drug dosage, by increasing the skin permeation rate of drug.
CN101851251B Dibutyltin (IV) complex for acyl hydrazone Schiff-base ligand and preparation method and application thereof The invention discloses a dibutyltin (IV) complex for an acyl hydrazone Schiff-base ligand. The complex has the following structural formula. The method for preparing the complex comprises the following steps of: adding 1mmol of o-vanillin-2-pyridineformyl hydrazone, 1 to 1.5mmol of dibutyl tin oxide, and 30ml of toluene-ethanol into a flask, and stirring and refluxing for 6 to 7 hours at the temperature of between 70 and 80 DEG C; after reaction, cooling to room temperature, and rotationally evaporating to obtain an orange-yellow solid; and recrystallizing by using dichloromethane-ethanol toobtain an orange-yellow transparent crystal, namely an organic tin complex. The dibutyltin (IV) complex for the acyl hydrazone Schiff-base ligand has high anti-cancer activity, and can prepare medicaments for treating liver cancer, lung adenocarcinoma, breast cancer, prostatic cancer, colon cancer or promyelocytic leukemia.
CN102114034A Novel compound rabeprazole composition The invention discloses a novel compound rabeprazole composition. The novel compound rabeprazole composition takes rabeprazole, sodium bicarbonate and magnesium hydroxide in a ratio of (0.5-2):37.5:17.15 as active components. In the composition, the rabeprazole comprises an optical isomer thereof and medicinal salt thereof. The optical isomer comprises levorotatory rabeprazole, dextrorotatory rabeprazole and racemic rabeprazole, wherein the dextrorotatory rabeprazole is preferred. The medicinal salt comprises sodium salt and magnesium salt, wherein the sodium salt is preferred. The novel compound rabeprazole composition can be combined with appropriate pharmaceutical excipients to form oral preparations which comprise granules, tablets, capsules, dispersible tablets, chewable tablets and the like.
CN102349929A Drug for treating and preventing fracture The invention discloses a drug for treating and preventing fracture, which is prepared by the ingredients of kelp, marine alga plant rich in algin and acetic acid or acetic anhydride. The preparation method of the drug is as follows: a, getting kelp and marine alga plant rich in algin, drying and grinding to powder, soaking the powder in acetic acid, wherein, the amount of the acetic acid added is in a standard that the acetic acid immerses the marine alga powder to carry out reaction for 2-3 weeks at normal temperature, pouring out the acetic acid liquid after the reaction is finished, drying under normal temperature, after drying, neutralizing through sodium hydroxide or other alkaline substance, after neutralizing, drying under normal temperature, and getting the substance used for preparing the drug for promoting fracture healing; and b, getting the kelp and the marine alga plant rich in the algin, drying and grinding to powder, soaking the powder in the acetic anhydride, the amount of the acetic anhydride added is in a standard that the acetic anhydride immerses the marine alga powder, then adding sulfuric acid for catalytic reaction, wherein the amount of the sulfuric acid added is 0.3% of the amount of the acetic anhydride, pouring out the acetic acid liquid after the reaction is over, drying under normal temperature, after drying, neutralizing through sodium hydroxide or other alkaline substance, after neutralizing, drying under normal temperature, and finally getting the substance used for preparing the drug for promoting fracture healing.
US7189758 2-Benzyl-2-hydroxy-4-methyl-4-phenylpentanoic acid (1-oxo-1,3-dihydroisobenzofuran-5-yl)amide for example; treating type II diabetes, obesity, hypertension, arteriosclerosis, or glaucoma A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
CN101590015B Cationic adhesion type mycophenolate mofetil nano eye drop The invention relates to a cationic adhesion type mycophenolate mofetil nano eye drop, which comprises mycophenolate mofetil of which the mass percentage concentration is 1 percent, proper amount of osmotic pressure modifying agent and pH modifying agent. The eye drop is characterized in that the eye drop also comprises chitosan, Pluronic F-68 and phospholipid, wherein the mass percentage concentration of the phospholipids in the eye drop is between 0.2 and 2 percent; the mass percentage concentration of the Pluronic F-68 in the eye drop is between 0.5 and 4 percent; the mass percentage concentration of the chitosan in the eye drop is between 0.5 and 4 percent; the molecular weight of the chitosan is between 5,000 and 300,000; the deacetylation degree is more than 85 percent; and the grain diameter of the mycophenolate mofetil is between 10 and 700 nm. The eye drop has the characteristics that: the mycophenolate mofetil with nanometer grain diameter improves the medicament solubility,the safety and the effectiveness; mycophenolate mofetil medicament particles are charged with positive charges so as to be favorable for improving the cornea absorption of the medicament, improving the medicament effect, prolonging the medicament duration, and greatly improving the cornea adhesion.
US8653257 Dibenzothiazepine derivatives and uses thereof—424 Compounds the following formula: wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds.
CN1879643A Pennogenic compound liquid molecular dispersible preparation The invention relates to a special preparation form with Pennogenin compounds as the active constituent, wherein the Pennogenin compound liquid state molecular dispersible preparation comprises the following constituents (by weight percent): Pennogenin compounds 0.5-20%, oil-wax mixture 80-99.5% comprising hydrogenated soybean oil 0.5-1.5 parts, yellow wax 0.5-1.5 parts, and short-chain vegetable oil 3-5 parts. The constituents can also include auxiliary solvent 1-20% and anti-oxidant 0.5-5%.
WO2010021930A1 Prevention and treatment of mrsa infections with chitosan-derivatives The present invention is directed to the treatment and prevention of nosocomial infections or MRSA infections utilizing soluble chitosan or chitosan derivative compounds. These chitosan-derivative compounds, e.g., chitosan-arginine and chitosan-acid amines, exhibit bactericidal activity against bacterial pathogens, e.g., drug resistant bacteria such as Methicillin-resistant Staphylococcus aureus (MRSA).
US20080207728 Bicyclic acyltryptophanols The present invention relates to acyltryptophanols of the general formula I, in which Q, V, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
WO2012175991A1 Fused pentacyclic anti - proliferative compounds The present invention relates to novel compounds of formula (I) wherein X, Q, R1, R2, R3, R4, R5, R6, R7, R8, R21, R22 and R23 are as defined herein. The compounds of formula (I) are inhibitors of telomerase enzyme function and are accordingly useful for the treatment cellular proliferation disorders, such as cancer.
US20080242715 Psychological disorders such as schizophrenia and sexual disorders The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein each group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; with the proviso that when m5=m6 =1, R7 is not chlorine; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents, premature ejaculation or cognition impairment.
EP2746284A1 Salt and polymorph of pyrazolopyrimidinone compound and drug composition, preparation method and use thereof The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.
CN101062054A Medicine for curing wound The invention relates to an externally-used medicament for treating trauma which is prepared from the following medicinal herbs (by weight ratio): sulfamethoxazole 30-40 parts, berberine 5-15 parts, calcined gypsum 15-30 parts, zinc oxide powder 15-20 parts.
CA2383372C Cell-specific and/or tumor-specific promoter retargeting of herpes gamma 34.5 gene expression The present invention relates to herpes viral mutants and methods of using these viral mutants for selectively targeting tumor cells or other populations of target cells. The viral mutants of the invention are capable of selective targeting due to the use of tumor-specific and/or cell-specific promoters to drive expression of the herpes .gamma.34.5 gene.
US20120108618 Thia-triaza-indacenes The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
US20090215732 Combination of compounds, which can be used in the treatment of respiratory diseases, especially chronic obstructive pulmonary disease (copd) and asthma The present invention provides pharmaceutical compositions comprising a glucocorticosteroid and a compound of formula: wherein m, R1, R2, R3, and R4 are as defined in the specification, and their use in therapy.
US20070197660 Compounds for modulating cell proliferation Compounds having the Formula (I) or (III) wherein R1, R2 and R3 are each independently selected from H, OH, C1-6alkyl, C1-6alkoxy, NH2, NH—(C1-6alkyl), N(C1-6alkyl)(C1-6alkyl), SH, S—C1-6alkyl, NO2, CF3, OCF3, and halo; R4 is unsubstituted Ar or Ar substituted with 1-4 substituents independently selected from C1-6alkyl, C1-6alkoxy and halo; X is selected from (CH2CH2O)n and (CH)n, and n=1-4, salts, solvates and hydrates thereof, useful for modulating or inhibiting cell proliferation, are described.
CN101991578A Application of asiatic acid and madecassic acid in preparation of alpha-glucosidase inhibitor drugs Asiatic acid and madecassic acid are extracted and prepared from Centella asiatica (L.) Urban, and pharmacological experiments prove that the asiatic acid and the madecassic acid have the activity of inhibiting alpha-glucosidase. The invention discloses a new use of the asiatic acid and the madecassic acid in the preparation of alpha-glucosidase inhibitor drugs, and the asiatic acid, the madecassic acid or a composition containing the asiatic acid and the madecassic acid can be used for preparing the alpha-glucosidase inhibitor drugs. The invention simultaneously discloses a new preparation method of the asiatic acid and the madecassic acid.
CN101816673A Medicinal preparation containing levodopa and cytidine diphosphate and application thereof in treating parkinson diseases The invention relates to a unit dosage combination preparation used for the combined delivery of levodopa and cytidine diphosphate or salts thereof. The preparation can be used for treating parkinson diseases. The invention also relates to a preparation method of the combined unit dosage preparation and a medical application of the combined preparation in treating the parkinson diseases.
CN103110582A Cannabinol compound micro-emulsion and preparation method thereof The invention relates to the field of pharmaceutic preparations and in particular relates to micro-emulsion containing a cannabinol compound. The micro-emulsion comprises the following components in percentage by weight: (a), 0.01wt%-30wt% of the cannabinol compound; (b), 0.01wt%-30wt% of oil phase, wherein the oil phase is selected from one or more of vegetable oil, fatty acid ethyl ester, fatty acid isopropyl ester, fatty acid glyceride and fatty acid polyethylene glycol glyceride; (c), 0.01wt%-60wt% of surfactant, wherein the surfactant is selected from one or more of polyoxyethylene ether castor oil, polyoxyethylene hydrogenated castor oil, poloxamer, fatty acid polyethylene glycol glyceride, polyoxyethylene dehrdrated sorbitol aliphatic ester and phospholipid; (d), 0.01wt%-40wt% of cosurfactant, wherein the cosurfactant is selected from one or more of alcohol, propylene glycol, isopropyl alcohol, polyethylene glycol, dimethyl isosorbide, isopropenyl carbonate, diethylene glycol monoethyl ether, tetrahydrofuran polyglycol ether and glycerol; and the balance being water or deionized water.
CN103230375A Mesalazine dripping pills and preparation method thereof The invention provides mesalazine dripping pills and a preparation method thereof. According to the invention, mesalazine and a substrate are combined according to a weight ratio of 1:1-100, such that the dripping pills are obtained. According to the invention, a mesalazine preparation form is changed from tablets unto dripping pills, such that the medicine is dispersed into the substrate in a state of molecules, colloid or microcrystalline. Medicine total surface area is increased. The substrate is hydrophilic, such that a wetting effect is provided for the medicine, and the medicine can be rapidly dispersed into micro-particles or solution. Therefore, medicine dissolving and absorption are accelerated, and bioavailability and medicine stability are improved. The dripping pills are highly efficient and convenient. Therefore, the mesalazine dripping pills provided by the invention has the advantages of accelerated dissolving and absorption, convenient application, high bioavailability and medicine stability, reduced adverse reaction, fast effect, convenient carrying, simple production process, and suitability for large-scale productions.
EP2752410A1 Heterocycle derivative having pgd2 receptor antagonist activity The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.
EP2583969A2 Novel rhodanine derivatives, method for preparing same, and pharmaceutical composition for the prevention or treatment of aids containing the rhodanine derivatives as active ingredients Disclosed are novel rhodanine derivatives which are inhibitory of HIV activity. Also provided are a method for preparing the novel rhodanine derivatives, and a pharmaceutical composition for the prevention or treatment of AIDS containing the rhodanine derivatives as active ingredients. Having high inhibitory activity against HIV, the rhodanine derivatives can be effectively used in the prophylaxis or therapy of AIDS.
CA2671776C Gal3 receptor antagonists for the treatment of depression This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and apharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.
WO2011109874A1 Inhibition of glutathione transferase zeta The present invention relates to a method for treating a metabolic condition in a subject, comprising administering a compound to said subject that inhibits the expression or activity of GSTZ or promotes degradation of GSTZ. The compound may inhibit or disrupt an interaction between GSTZ and one or more molecules, compounds or cellular components.
CN1586462A New use of glutaraldehyde in preparing aminal medicine The present invention relates to the new use of glutaraldehyde in preparing animal medicine for digestive tract administration to treat animal's disease caused by pathogenic microbe via digestive tract infection. The present invention is proposed and completed based on one known microbiological principle. The medicine of the present invention is superior to available antiviral and antiseptic medicines and has the advantages of wide treating spectrum, fast and determined effect, small dosage, no resistance, no medicine residue, etc.
US20110172301 Use of anti-oxidant compounds for muscle recovery The present invention describes the use of a composition comprising a compound according to formula (1) to retain or restore muscle health: formula (1) wherein: R can be H, OH or CH3O; R1 can be H, (CH2)nOR2 wherein: n is 1, 2 or 3 R2 is H, COCH3 or formula (2) wherein m is 1, 2 or 3 with the proviso that R and R1 are not H at the same time. The invention furthermore relates to the use of a compound according to formula (1) in the manufacture for a composition to retain or restore muscle health, thereby for example preventing and/or treating muscle damage due to exercise. More specifically, such composition includes food, beverages, supplements and feed.
US20050090525 carboxymethylated N-(nitrogen group functionalized alkyl- carbonylhydrazido)- or carbonylaminomethylcarbonyl)- substituted; integrin inhibitors used for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammation, tumors, osteoporosis, infections and restenosis Isoquinoline derivatives of the general formula (I) in which X, Y, Z, R1, R2, and n are as defined in Patent Claim (1), and physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammation, tumours, osteoporosis, infections and restenosis after angioplasty or in pathological processes which are maintained or propagated by angiogenesis.
WO2013164711A1 Anti-adherent formulation including a cationic or nonionic acrylate co-polymer Liquid formulations having anti-adherent properties are disclosed herein. The liquid anti-adherent formulation described herein acts to prevent the adherence of menses and/or fecal material to the skin in the labial and perianal regions during and after menstruation or defecation, respectively. The liquid anti-adherent formulation contains a carrier, a polymer selected from a nonionic acrylate co-polymer, cationic acrylate co-polymer, and combinations thereof. Anti-adherent formulation is found to be effective if a menses leave on percentage as defined within the Menses Leave-On Percentage Test method described herein was less than 6.2% after two insults.
DE102009042459A1 Composition, useful for the treatment and prophylaxis of diseases of the liver, cardiovascular disease, dementia and Alzheimer's disease, comprises colloidal silver, gold and/or platinum and a choline-containing phosphoglyceride Composition comprises colloidal silver, gold and/or platinum and at least one choline-containing phosphoglyceride (I). Composition comprises colloidal silver, gold and/or platinum and at least one choline-containing phosphoglyceride of formula (R1-CH(R3)-CH(R2)-CH 2-O-P(=O)(O ->)-O-CH 2-CH 2-N +>(CH 3) 3) (I). R1, R2 : H, OH, R4-COO- or R4-CONH; R3 : H or OH; and R4 : any optionally saturated carbon residue having 6-26C. An independent claim is included for a pharmaceutical composition comprising the above composition and optionally other auxiliaries and additives. - ACTIVITY : Hepatotropic; Cardiovascular-Gen.; Nootropic; Neuroprotective. - MECHANISM OF ACTION : None given.
US20110098295 Methods of treating anxiety, itching and psychiatric disorders A method of treating an undesirable AC8-related condition in a mammal is provided comprising the step of inhibiting AC8 in the mammal
EP2755635A1 Aqueous compositions comprising arbekacin The invention provides aqueous liquid pharmaceutical compositions comprising arbekacin and chloride ions. The compositions are well tolerable for use in a method for treatment or prevention of a disease of the upper or lower respiratory tract, wherein the composition is aerosolized and inhaled by the patient. Furthermore, the invention provides arbekacin hydrochloride.
CN101857642B Polysaccharide derivative and vanadium complex application thereof The invention discloses a preparation method of a polysaccharide derivative and vanadium complex, which comprises the following steps of: firstly, reacting NaOH-alkalifying polysaccharide with chloroacetic acid for 3-4 hours at the temperature of 40-80 DEG C to synthesize the polysaccharide derivative; then reacting the polysaccharide derivative with a vanadium solution for 12-24 hours at the room temperature to obtain the vanadium complex of the polysaccharide derivative. The polysaccharide derivative and vanadium complex is applied to medicines for treating diabetes mellitus. In the invention, the polysaccharide derivative is adopted as raw material and reacts with VOSO4 in an aqueous medium under the neutral condition to obtain the polysaccharide derivative and vanadium complex throughfiltration, drying and crushing. In the invention, the complex preparation is completely carried out at the room temperature, has simple process and is easy to realize industrial production.
CN103462908A Rabeprazole sodium freeze-dried powder injection for injection and preparation method thereof The invention discloses a rabeprazole sodium freeze-dried powder injection for injection. The admixture in the freeze-dried powder injection comprises tromethamine; and the tromethamine is prepared into liquor and freeze-dried to obtain the freeze-dried powder injection. The freeze-dried powder disclosed by the invention has the advantages of high stability, fewer varieties of adjuvants and higher preparation safety; and the technique is simple and suitable for the requirements of mass production.
CN103301467A Stable taste-masking ambroxol hydrochloride compound and preparation method thereof The invention relates to a stable taste-masking ambroxol hydrochloride compound and a preparation method thereof. The medicine compound comprises ambroxol hydrochloride and a taste-masking agent, wherein the taste-masking agent is polacrilex IRP64, polacrilin potassium IRP88 and sodium polystyrenesulfonate IRP69. The medicine compound is selectively added with other pharmaceutically acceptable auxiliary materials to be further prepared into granules, chewable tablets, orally disintegrating tablets, oral cavity dispersion film agents and the like; the stable taste-masking ambroxol hydrochloride compound is pleasant in mouth feel, rapid to absorb, stable in quality, and simple and feasible in preparation process, the large-scale production is realized by using regular pharmaceutical equipment.
CN102302512A Multi-vitamin mineral tablet The invention relates to the field of medicine, and discloses a multi-vitamin mineral tablet. The multi-vitamin mineral tablet is composed of a vitamin layer, an isolation layer and a mineral layer, wherein the isolation layer is positioned between the vitamin layer and the mineral layer, and has the thickness of 1-2mm; and the vitamin layer contains vitamin C. According to the invention, vitaminand mineral elements are isolated effectively by utilizing the isolation layer between the vitamin layer and the mineral layer, vitamin C is protected effectively, the use amount and variety of the auxiliary materials are not required to be increased additionally, and the production cost is lower.
US20080214573 Compounds Useful for Inhibiting Chk1 Substituted urea compounds useful in the treatment of diseases and C1-3alkyleneOR3 conditions related to DNA damage or lesions in DNA replication are disclosed formula (I), wherein X1 is null, —O—, —S—, —CH2—, or —N(R1)—; X2 is —O—,. -£>.-, or —N(R1)—, -.. Y xs 0 or S; or =y represents two hydrogen atoms attached to a common carbon atom, —W is selected from the group consisting or heteroaryl, aryl, heterocycloalkyl, cycloalkyl, and C1-6alkyl substituted with a heteroaryl, or aryl group; R6 is —C≡C—R7 or heteroaryl; R8, R9, and R10, independently, are selected from the group consisting of halo, optionally substituted C1-6alkyl, C2-6alkenyl, C2-6alkynyl, OCP3, CF3, NO2, CN, NC, N(R3)2, OR3, CO2R3, C(O)N (R3)2, C(O)R3, N(R1)COR3, N(R1)C(O)OR3, N(R8)C(O)OR3, N(R1)C(O)C1-3alkyleneC(O)R3, N(R1)C(O)C1-3alkyleneC(O)OR3, N(R1)C(O)C1-3alkyleneOR3, N(R1)C(O)C1-3alkyleneNHC(O)OR3, N(R1)C(O)C1-3alkyleneSO2, NR3, C1-3alkyleneOR3, and SR3; Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed
US20080311185 Deregulated Genes and/or Processes in Inflammatory Arthritis The invention provides means and methods for determining whether a sample is derived from an individual suffering from inflammatory arthritis or from an individual at risk of suffering there from, said method comprising measuring in said sample the level of expression of at least one gene product of a gene of table A, table B or and comparing said expression level with a reference value. Further provided is a non-human animal model comprising an altered expression of a gene of table A, table B or when compared to a reference non-human animal, and use of this model as or in an arthritis model. Further provided is an in vitro assay for screening compounds for effect on a phenotype of synovial fibroblasts. The synovial fibroblast are preferably derived from a human or non-human animal suffering from inflammatory arthritis.
WO2009006787A1 Composition comprising rotigotine, its use and transdermal patch comprising the composition The invention discloses a composition comprising rotigotine and use of it for manufacturing transdermal patch comprising rotigotine. The composition is based on a mixed matrix consisting of acrylic-type pressure sensitive adhesive, siloxane-type pressure sensitive adhesive and polyvinyl pyrrolidone with certain weight ratio, in which (1) acrylic-type pressure sensitive adhesive is present in about 1-25% by the weight of said matrix; (2) siloxane-type pressure sensitive adhesive is present in about 65-98% by the weight of said matrix; (3) polyvinyl pyrrolidone is present in about 1-10% by the weight of said matrix; and rotigotine is about 1-40% by weight based on the weight of the total composition. The invention also discloses a transdermal patch comprising the composition of rotigotine. The patch provides improved good nature of solubility, delivery and initial drug flux of rotigotine.
EP1747781A1 Stable oral pharmaceutical preparation comprising fosfomycin, which is intended for diabetic patients The invention relates to a pharmaceutical preparation for the oral administration of fosfomycin in powder or granule form for a solution comprising an excipient system that is compatible with the active principle, which does not pose any risk of undesirable colour formation and which is suitable for administration to diabetic patients. The excipient system comprises mannitol and/or xylitol and an artificial sweetening agent which is selected from the group including: acesulfame, aspartame, saccharin, alitame and/or cyclamate.
CN1778301A Budesonide target-direction microball and preparation thereof A colon-target micropill of budesonide is disclosed. Its preparing process features that the beta-cyclodextrins is used to prepare the hydrophilic precursor from the water-insoluble budesonide, and the water-soluble coating is then used.
CA2702356C Pharmaceutical formulation comprising a proton pump inhibitor for the treatment of gastrointestinal conditions independent of food intake The present invention relates to a method of treating a gastrointestinal disorder by administering to a patient in need of treatment thereof a pharmaceutical composition, wherein said pharmaceutical composition can be administered to the patient independent of the intake of food.
WO2012020123A3 Neuropilin as a biomarker for bevacizumab combination therapies The present invention provides methods for improving treatment effect in a patient suffering from gastric cancer, in particular, adenocarcinoma of the stomach or gastro-esophageal junction ("GEJ"), by treatment with bevacizumab (Avastin®) in combination with a chemotherapy regimen by determining the expression level of neuropilin relative to a control level determined in patients suffering from gastric cancer, in particular, adenocarcinoma of the stomach or gastro-esophageal junction ("GEJ"). The improved treatment effect may be improved overall survival or improved progression free survival. The present invention further provides for methods for assessing the sensitivity or responsiveness of a patient to bevacizumab (Avastin®) in combination with a chemotherapy regimen, by determining the expression level of neuropilin relative to a control level determined in patients suffering from gastric cancer, in particular, adenocarcinoma of the stomach or gastro-esophageal junction ("GEJ").
EP2403533A1 Methods of enhancing peroxide activity Skin is treated by applying a composition including an organic peroxide to an area of the skin and then exposing the area of skin to an energy source.
WO2009152430A2 Methods of treatment of bipolar disorder A method of treating an individual diagnosed with bipolar disorder, comprises determining the number of manic episodes and/or depressive episodes experienced by an individual exhibiting one or more symptoms of bipolar disorder (e.g., bipolar disorder I); and if the number of manic episodes and/or the number of depressive episodes is each 2 or greater (e.g., 3 or greater, 4 or greater, 5 or greater, 6 or greater, 10 or greater, or 15 or greater), administering to the individual an effective amount of a uridine composition.
CN103732586A Acetyltanshinone IIA (ATA) as anticancer agent The present invention relates to the use of a compound of Formula I for the manufacture of a medicament for treating or preventing cancer in a subject.
WO2006092710A1 Metabolites of 2-{3-[4-(2-isopropoxyphenyl) piperazin-1-yl]-propyl}-3a,4,7,7a-tetrahydro-1h-isoindole-1,3-(2h)-dione The present invention relates to the metabolites of 2-{3-[4-(2-isopropoxyphenyl) piperazin-1-yl]-propyl}-3a,4,7,7a -tetrahydro-1H-isoindole-1,3(2H)-dione of Formula I. The disclosed compounds can function as 1a-adrenoceptor antagonists and thus can be used for the treatment of benign prostatic hyperplasia (BPH) and related symptoms thereof. Processes for preparing the metabolites, pharmaceutical composition containing these metabolites and the method of treating BPH and related symptoms thereof are also provided.
CN101669996B Method for preparing vision-health buccal tablet The invention belongs to the field of nutritional health food and particularly relates to a method for preparing vision-health buccal tablets. The buccal tablet mainly comprises the following components: bilberry, mulberry, natural red apatococcus lobatus, corn mint, chrysanthemum, lutein, vitamin A, honey and dextrin. The method comprises the steps of mixing and crushing the components, adding water in the components for refluxing, clarifying and filtering the mixture, condensing, granulating, drying, pressing and sterilizing the mixture, thus obtaining the finished product. As the effectivecomponents such as anthocyanin, astacin and the like are contained in the buccal tablet, the component combination in the compounding also has extremely obvious effect on vision protection, the raw materials are obtained from natural materials, the honey is taken as the sweetener in the product, thus improving the taste and leading the buccal tablet to be easy to be accepted.
WO2011140128A2 Nail discoloration and fungus treatment A system and method for treating human nails afflicted with fungus, discoloration, or which are unusually thick is now disclosed. The system comprises a hydrogel moist pad or pad, a treatment agent comprising a metallic colloidal suspension having antifungal activity in an aqueous environment, and an adhesive for securing the hydrogel and treatment agent to a nail in need of such treatment. A method and regimen for treatment of the nail is also disclosed.
CN103432590A Graphene quantum dot nuclear targeting medicine carrying system as well as preparation method and application thereof The invention discloses a graphene quantum dot nuclear targeting medicine carrying system as well as a preparation method and application thereof. The preparation method comprises the following steps: firstly, sterilizing an aqoeous solution of a graphene quantum dot and an aqoeous solution of an anti-cancer medicine; secondly, mixing the aqoeous solution of the graphene quantum dot and the aqoeous solution of the anti-cancer medicine according to the mass ratio of (5:1)-(50:1) to obtain a medicine carrying system; thirdly, co-cultivating the medicine carrying system and cells, detecting the toxicity of the cells by using an MTT (Methyl Thiazolyl Tetrazolium) method and detecting a medicine loaded into the cells by using a fluorescent microscope. According to the invention, by virtue of the characteristic that the graphene quantum dot has a single-atom planar structure, the graphene quantum dot and a micromolecule anticancer medicine with a polycyclic planar structure are combined by bonds to form the medicine carrying system which can stably exist in the aqoeous solution. The graphene quantum dot has a medicine carrying function; meanwhile, the graphene quantum dot has a special structure, so that the toxicity of the medicine to the cells can be increased. The medicine carrying system has the advantages of lower toxicity, simple preparation method, easiness for implementation and double functions of carrying the medicine and enhancing the toxicity of the medicine to the cells.
EP2467147A1 Novel multi purpose composition The present invention relates to a novel multi purpose composition and process of its preparation. This composition comprises lime stone and processed navasar.
US20100069436 Imidazole compounds having an antiinflammatory effect The invention relates to imidazole derivatives of the Formula (I) in which the radicals R1, R2, R3, R4 and R5 have the meanings indicated in the description. The compounds of the invention have an immunomodulating and/or cytokine release-inhibiting effect and are therefore suitable for the treatment of disorders associated with an impairment of the immune system.
WO2009117156A1 Pyrazolo-pyrazinone compounds and methods of use thereof The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I) wherein A1, B, R1, R2, R3, R4, R5 and n are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).
CA2085785C The use of 4-aminopyridine in the treatment of a neurological condition The use of 4-aminopyridine to treat a neurological condition is described. In particular, the present invention relates to the use of 4-aminopyridine to treat spinal cord injured individuals. It has been found that 4-aminopyridine can reduce pain and spasticity in a spinal cord injured individual when given in doses from about 18 to about 30 milligrams intravenously. The results are quite significant due to the high incidence of these problems and the intractable nature of central pain in the spinal cord injured individuals. 4-Aminopyridine is also useful in increasing sensory ability and motor control.
CN101585835A Preparation method and application of bencycloquidium bromide optical isomer and composition of bencycloquidium bromide optical isomer The invention relates to the technical field of medicaments, in particular to a preparation method and application of a bencycloquidium bromide optical isomer. The isomer is obtained by a chemical resolution method, the activity of the isomer is far beyond that of other isomers and racemic forms; when the isomer is taken as a medicament to be taken, the taking dosage is reduced, and side effects caused by other isomers are simultaneously eliminated; moreover, the bencycloquidium bromide optical isomer has a romurtide cyclodextrin inclusion compound with higher pharmaceutical value and a preparation thereof. The romurtide is coated by the cyclodextrin, so that the problems of low water-solubility, unstable preparation prepared by the romurtide cyclodextrin inclusion compound and the like are solved. The romurtide cyclodextrin inclusion compound has the characteristics of high stability, good water-solubility, and low toxic and side effects, and is a quite good immunomodulator.
CN102138929A Surgical hemostat for pets and preparation method thereof The invention relates to a surgical hemostat for pets and a preparation method thereof, and belongs to the technical field of medicines. A molecular formula of the hemostat is -[(CH2-CHCOOH)n-(CH2CHOOFexl/x)]-m, wherein in the formula, n is equal to 150 to 40,000, x is equal to 2 or 3, and m is equal to 50 to 500. The preparation method comprises the following steps of: heating solution of crylic acid, adding K2S2O8, stirring at the temperature of between 80 and 85 DEG C for reacting for 50 to 80 minutes, and cooling; diluting by water, adding ferrous sulfate, and stirring for reacting; and removing low polyacrylic acid and sulfate radicals by using a semipermeable membrane, and drying to remove moisture. The surgical hemostat for the pets is prepared by a simple method, and has low cost, excellent hemostatic effect and short hemostatic time, and the good inhibitory effect on common infectious bacteria in the pets.
EP2768504A1 Compositions for controlling vascularization in ophthalmological and dermatological diseases A treatment method for controlling vascularization in a patient's eye or skin includes administering to the patient's eye or skin a pharmaceutical composition having formula (I) or a pharmaceutically acceptable salt, hydrate, enantiomer, diastereomer, racemate or mixtures of stereoisomers thereof. wherein the patient has a disease or disorder associated with vascularization in the eye or skin or wherein said patient is at risk for developing a disease or disorder associated with vascularization of the eye or skin.
WO2009087615A1 Pharmaceutical compositions and methods utilizing a d-amino acid and an antioxidant for treating neuropsychiatric disorders The present invention provides a pharmaceutical composition for oral administration comprising a D-amino acid combined with an antioxidant selected from the group consisting of vitamin E, vitamin C, a glutathione or a precursor thereof.
CN103371998A Application of Chukrasone B in preparation of medicines for preventing or treating renal insufficiency The invention discloses an application of Chukrasone B in the preparation of medicines for preventing or treating renal insufficiency, and belongs to the technical field of new applications of medicines. The application of the Chukrasone B in the preparation of medicines for preventing or treating renal insufficiency is disclosed by the invention for the first time. As the skeleton type of the Chukrasone B belongs to a bran-new skeleton type and the Chukrasone B has unexpected strong inhibitory activity on renal insufficiency, the possibility that other compounds provide revelation does not exist. The Chukrasone B has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for preventing and treating the renal insufficiency.
CN102973644A Drug for treating acute or chronic hepatitis, and preparation method thereof The invention relates to the field of drug preparation and discloses a drug for treating acute or chronic hepatitis, and a preparation method thereof. The preparation method is characterized by comprising the following steps: extracting, concentrating and purifying active ingredients to radix sophorae tonkinensis, drying, and granulating to prepare into tablets or granules or hard capsules through filling. The preparation method is simple to operate, low in cost, easy for the process to control, and pollution-free. The prepared drug is obvious in curative effect on patients with acute or chronic hepatitis, and can fast lower aminotransferase.
CN1568987A Dripping pills of paroxetine hydrochloride and its preparation method The invention relates to an Paroxetine Hydrochloride drop pill prepared by utilizing ultramicro disintegration and drop pill manufacturing process, which has the advantages of improving collapse and dissolving speed, dissolving out speed and degree, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use. oral or swallow administration, It has good compliance, thus is especially suitable for children, the elderly, bedridden patients and dysphagia patients.
EP1461037B1 Process for preparation of a beverage treated with a nicotine containing substance A beverage for suppressing the urge to smoke is made by heating a mixture of water and a substance containing nicotine. Thereafter the mixture is filtered to produce a beverage which has no discernible taste, smell or appearance of nicotine.
US20070032487 Inhibitors of phosphatidylinositol 3-kinase Compounds of formula I in free or salt form, wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
CN102234260A C-aryl glucoside derivatives containing difluoromethylene group The invention relates to C-aryl glucoside derivatives containing a difluoromethylene group. Specifically, the invention provides novel sodium-dependent glucose transporter (SGLT-2) inhibitors, a preparation method thereof and application thereof in preparing drugs for the treatment of diseases related to SGLT-2, especially diabetes, obesity and diabetic complications. The C-aryl glucoside derivatives provided by the invention have stronger inhibition activity and higher selectivity for sodium-dependent glucose transporter (SGLT-2), and can obviously promote the emission of glucose in urine of animals.
WO2007135766A1 Ointment for amelioration or treatment of oral tumor The purpose is to provide an ointment for leukoplakia or oral cancer, which contains a substance derived from a natural product as an active ingredient, is highly safe, and can be used over a prolonged period. Disclosed is an ointment for the amelioration or treatment of oral tumor, which comprises a green tea leaf extract and alginic acid or a salt thereof. Also disclosed is a beverage/food containing the ointment.
WO2014079364A1 Imidazolone derivatives, pharmaceutical compositions and uses thereof Imidazolone compounds, pharmaceutically acceptable salts, solvates, polymorphs or prodrugs thereof are disclosed. Pharmaceutical compositions comprising above substances and uses for preventing and treating protein kinases related diseases, such as cancers, metabolic diseases, cardiovascular diseases and the like, are also disclosed.
WO2008112646A1 Aminopyridines useful as inhibitors of protein kinases The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
CN102584830A Dihydroindene amide compounds, and medicinal composition and application thereof The invention relates to dihydroindene amide compounds with a structure shown as a formula (I) or pharmaceutically-acceptable salt of the compounds, polymorphic substances of the compounds, solvates or prodrugs of the compounds, a medicinal composition containing the compounds and application of the compounds or the medicinal composition to the preparation of medicines for treating or preventing diseases or imbalance relevant to the activity of protein kinase or the abnormality of cell proliferation.
US20110135641 Radioprotectants targeting thrombospondin-1 and cd47 Described herein is the discovery that cell and tissue survival can be dramatically increased following radiation exposure through inhibition of the interaction between TSP-1 and CD47. This effect is shown using antisense molecules, peptides, and antibodies, which can now be used as radioprotectant agents. These agents find application in minimizing, reducing and/or preventing tissue damage following intentional and accidental radiation exposure, as well as increasing the therapeutic efficacy of radiation therapies by protecting non-target tissue from incidental radiation damage and by increasing tumor ablation following radiation treatment.
US20120251566 Saponin adjuvant compositions and methods relating thereto An adjuvant composition which comprises an anionic macromolecule component particularly an ionic polysaccharide such as DEAE-dextran, and a saponin component, particularly an immunostimulating complex component. Immunogenic compositions comprising an immunogen and this adjuvant composition are also disclosed together with methods of use thereof.
US20100129363 Methods and compositions using pde4 inhibitors for the treatment and management of cancers Methods of treating, preventing and/or managing hematological cancers are disclosed. Specific methods encompass the administration of a PDE4 inhibitor alone or in combination with a second active agent. The invention further relates to methods of treating leukemias and lymphomas which comprise the administration of a PDE4 inhibitor. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
CN102898332A Hydroxamic acid derivative, its pharmaceutical composition, preparation method and application The invention belongs to the pharmaceutical chemicals field, and relates to a hydroxamic acid derivative, its pharmaceutical composition, a preparation method and an application. The invention relates to a compound shown in a formula I or a formula II, or its pharmaceutical salt. The compound can effectively adjust the activity and/or level of CLA-1, and has a prospect for preventing and treating cardiovascular and cerebrovascular diseases (such as atherosclerosis).
CN103751217A Propolis-containing compound preparation The invention provides a propolis-containing compound effervescent preparation, which can be used as medicament, health-care food or food and is used to prevent osteoporosis, menopausal syndrome and cardiovascular diseases, maintain the health and beauty of women and delay aging. Propolis-containing natural plant extract is proportioned with vitamins, amino acids and trace elements in a certain ratio, mixed with auxiliary materials including an effervescent agent, an adhesive and a lubricant, and processed through a specific process into effervescent tablets or effervescent granules. The preparation has the advantages of fully maintaining the biological activity of active ingredients, promoting the absorption of active ingredients in human bodies, providing convenience for taking, and the like.
US20080261906 Screen for agents that modulate replication of hepatitis C virus; detect binding modulators of TBC and NS5A, inhibition of TBC activity, inhibition of Rab1 activity, expression of the TBC protein and/or Rab1 protein The invention features methods and compositions for screening for agents that modulate replication of a virus, particularly Flaviviridae virus (particularly hepatitis C virus (HCV)), where the methods provide for detection of agents that modulate the binding of TBC and NS5A, the inhibition of TBC activity, inhibition of Rab1 activity, and/or the expression of the TBC protein and/or Rab1 protein. The invention also features methods of controlling viral replication, and agents useful in such methods.
EP1829874A1 Tricyclic compound and use thereof The present invention relates to the compound represented by formula (I): (wherein, all the symbols has the same meanings as that of the specification.), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.
CN103127064A Application of Eryngiolide A in respiratory syncytial virus medicines The invention discloses application of Eryngiolide A in respiratory syncytial virus resisting medicines. Experiment result shows that the Eryngiolide A has evident inhibiting effect on respiratory syncytial virus (RSV). The application of the Eryngiolide A in the respiratory syncytial virus resisting medicines provides experimental base for clinically curing infectious disease with the RSV, provides certain guiding significance for developing the respiratory syncytial virus resisting medicines, and has important reference value.
CN102068452B Antiviral medicinal composition The invention relates to a synergic antiviral medicinal composition, which contain baicalein and ribavirin in a weight ratio ranging from 20:1 to 1:10. The medicinal composition has the advantages of low medicament tolerance, fewer side effect and adverse effects, and the like. In addition, the medicinal composition has the function of inhibiting the duplication of viruses, and has outstanding advantages and a bright development prospect in preventing and treating influenza viruses.
US20080108643 synergistic mixture of Memantine derivatives (5 - 20 mg per day) and dextromethorphan (15 - 30 mg); Pervasive Developmental Disorders (PDD); sensory integration problems, verbal and non-verbal communication, social interactions, and leisure or play activities; side effect reduction A method for treating autism comprising the step of administering an effective amount of Memantine and dextromethorphan or pharmaceutically acceptable derivatives and/or salts thereof.
CN103356545A Application of Sarcaboside B in medicine used for treating ovarian cancer The invention discloses an application of Sarcaboside B in preparation of a medicine used for treating ovarian cancer and belongs to the technical field of new applications of medicines. In vitro MTT (methyl thiazolyl tetrazolium) antineoplastic activity evaluation shows that Sarcaboside B has an obvious inhibiting effect on growth of human ovarian cancer cell strains such as HO-8910, HOC1 and OVAC, so that Sarcaboside B can be used for preparing an anti-ovarian-cancer medicine and has a good development application prospect; the application of Sarcaboside B in preparation of the medicine used for treating ovarian cancer is disclosed for the first time, a brand new skeleton type is adopted, and Sarcaboside B has an unexpected inhibitory activity on human ovarian cancer cells.
US7592354 Administering a stimulantfor the endogenous production/ release of somatotropins; 3-((1-(2-aminoprop-2-yl)carbonylamino-),2-(phenylmethoxymethyl-)ethyl-),5-(morpholino-carbonyloxymethyl-)-5,6,7,8-tetrahydro-1,2,4-triazolo(4,3-)pyridine; osteoporosis; obesity;improving bone densisty, muscle mass/strength Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1′, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
WO2008073752A3 Cyclobutyl derivatives for the treatment of glaucoma Compound having the formula below are disclosed herein:formula (I).Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
US20100247455 Periodontal Bacterial Growth Inhibitor, Oral Hygiene Product, and Food and Drink A periodontal bacterial growth inhibitor contains as an active ingredient a Macaranga tanarius extract extracted from Macaranga tanarius with an extraction solvent including at least an organic solvent. Alternatively, the periodontal bacterial growth inhibitor contains as an active ingredient at least one selected from nymphaeol-A, nymphaeol-B, and nymphaeol-C. The periodontal bacterial growth inhibitor is used by being blended to, for example, an oral hygiene product or a food and drink.
EP1085862B1 Treatment of an autoimmune disease A method of administering an amino acid protocol intravenously for the treatment of a patient suffering from an autoimmune disease is provided.
CN102038732A Cream for treating acne The invention relates to cream for treating acne. The cream is characterized in that the cream is prepared from the following raw materials in weight ratio: sublimed sulfur, borax, berberine, ofloxacin, safflower, cimetidine, propolis, dimethyl sulfoxide and pure cream. The medicaments are combined skillfully to generate synergy. The cream is coated on an affected part for two to three times every day, and can diminish inflammation and swelling, inhibit fat, care skin, quickly kill bacteria, eliminate rash, relieve itching, quickly recover the injured sebaceous gland tissues and quickly recover the function of the skin. The affected part can be healed in 1 to 4 weeks, and no scar is left after healing. The cream is simple for treatment and convenient to use, and has low cost, no pain, safety and reliability.
US20110020317 Breast tumour grading We describe a method of assigning a grade to a breast tumour, which grade is indicative of the aggressiveness of the tumour, the method comprising detecting the expression of a gene selected from the genes set out in Table D1 (SWS Classifier 0).
CN102234231A 1-substituted-2-substituted-4- aryl substituted-butyl-2-alkene 1, 4-diketone compound, its preparation method and application The invention discloses a 1-substituted-2-substituted-4- aryl substituted-butyl-2-alkene 1, 4-diketone compound, or its isomers, pharmacy-acceptable salts, preparation method and applications, and medicine compositions containing the compound. The protein-tyrosine phosphatase 1B inhibition test proves that the compound has good inhibitive activity of PTP1B, and can be used for treating diabetes mellitus, obesity and complications triggered by diabetes mellitus and obesity.
WO2006113498A3 2-amino-quinaz0lin-5-ones as hsp90 inhibitors useful in treating proliferation diseases 2-Amino-quinazolin-5-one compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cell proliferative diseases.
EP2425841A1 Methods Employing and Compositions Containing Defined Oxidized Phospholipids for Prevention and Treatment of Atherosclerosis Novel synthetic forms of etherified oxidized phospholipids and methods of utilizing same for preventing and treating atherosclerosis and other related disorders are provided. In addition, methods of synthesizing esterified oxidized phospholipids and using same for preventing and treating atherosclerosis and other related disorders are also provided.
US20080020993 Regulation of cell proliferation and differentiation using topically applied nucleic acid molecules Methods are disclosed for the regulation of cell differentiation and proliferation, e.g., for treating hyperproliferative skin disorder, such as psoriasis, and skin cancer for enhancing wound healing, for stimulating hair growth and inhibiting hair growth, by administration of nucleic acid molecules encoding parathyroid hormone (PTI), parathyroid related peptide (PTHrP), or fragment, analog or derivative thereof, and salts thereof, encapsulated by particular liposomes or incorporated into a porous biocompatable matrix.
CN1739575A Solid and liquid attapulgite prepn for treating digestive tract diseases The present invention belongs to the field of medicine preparation technology, and natural attapulgite is used as the active component for treating acute and chronic diarrhea, enteritis and other digestive tract diseases. Attapulgite as one natural mineral is hard, great in specific surface area and hard to process. The present invention prepares attapulgite capsule, tablet, granule and gel through solving relevant technological problems in tabletting, encapsulating, etc. and the preparations have the physiological activity maintained.
US20100104522 Compostion for skin external use containing omega-3 fatty acid Stable preparations containing omega-3 fatty acid as an effective ingredient are disclosed. Further, uses of omega-3 fatty acid in preventing or alleviating skin aging, moisturizing skin, improving skin roughness, restoring or strengthening skin barrier function, improving skin elasticity, recovering or preventing skin damage induced by UV are disclosed.
WO2007021234A1 Boron compounds useful in bnct The present invention relates to novel boron-comprising compounds, to pharmaceutical compositions comprising said compounds, to the therapeutic use of said compounds, and to a process for preparation of said compounds. The compounds are useful in boron neutron capture therapy (BNCT).
EP1562958B1 N-sulfonylaminothiazole N-(4,5,6,7-tetrahydro-thiazolo-[5,4-c]pyridin-2-yl)-(C6-18)arylsulfonamides, wherein the nitrogen atom of the pyridine is substituted, and wherein the pyridine ring is optionally bridged, useful as a pharmaceutical related to steroid sulfatase.
WO2007049532A1 Aminodihydrothiazine derivative A BACE 1 inhibitor containing, as an active ingredient, any one of a compound represented by the formula (I): (wherein ring A is an optionally substituted carbocyclic group or optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1 (R1 is hydrogen or lower alkyl); R2a, R2b, R3a, R3b, R4a, and R4b each independently is hydrogen, halogeno, hydroxy, etc.; n and m each independently is an integer of 0-3, provided that n+m is 1-3; and R5 is hydrogen, optionally substituted lower alkyl, etc.), a pharmaceutically acceptable salt thereof, and a solvate of either.
EP2245012A1 Inhibitors of p38 map kinase Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is -N= or -CH=; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5 - 13 ring members; R6 is hydrogen or optionally substituted CrC3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula (IA); wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5 - 13 ring members; z is O or 1; -X1-L1-Y- is a linker radical or bond; R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 are as defined in the claims.
US20100240720 Allosteric jnk inhibitors The disclosure provides compounds and compositions, and methods of using these compounds and compositions, for the targeted delivery of chemotherapeutic agents.
WO2005097775A1 Piperidine derivates for the treatment of chemokines mediared disease The present invention provides a compound of a formula (I) wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
WO2013140319A9 Crystalline form of a succinate salt This invention relates to a new crystalline form of the succinate salt of the epithelial sodium channel (ENaC) blocker 3-(3-{2-[(E)-3,5-Diamino-6-chloro-pyrazine-2-carbonylimino]-1,3,8- triaza-spiro[4.5]decane-8-carbonyl}-benzenesulfonylamino)-propionic acid dipropylcarbamoylmethyl ester, pharmaceutical compositions comprising said crystalline form, uses of said crystalline form and pharmaceutical compositions, and methods for preparing said crystalline form.
WO2009100955A1 Antisense rna targeting cxcr4 MiR-146a and antagomirs thereof are useful in controlling expression of CXCR4 and megakaryopoiesis, tumor metastasis, HTV entry and/or Rheumatoid Arthritis.
CN1736384B Mixture of higher primary aliphatic alcohols with acetylsalicylic acid and pharmaceutical formulation The present invention relates to a pharmaceutical preparation containing the following mixtures and use thereof, as well as use of the following mixtures. A mixture of higher primary aliphatic alcohols of 22 to 38 carbon atoms can be obtained by saponifying and extracting steps with organic solvents from sugar cane wax. The mixture which contains tetracosanol, hexacosanol, heptacosanol, octacosanol, nonacosanol, triacontanol, dotriacontanol and tetratriacontanol can be used for the treatment of hypercholesterolemia, and atherosclerotic complications as platelet hyperaggregabiulity, ischemia and thrombosis, and prevents drug induced gastric ulcer and improves male sexual activity.
US20100160389 Dihydropyridone amidesas p2x7 modulators Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
CN102133201A Faropenem sodium freeze-dried powder injection The invention relates to a Faropenem sodium freeze-dried powder injection, which comprises only one composition: Faropenem sodium. Preferably, injection water is added into Faropenem sodium powder with the particle size of 75 to 100mum to be prepared into Faropenem sodium solution with concentration of 5-20 percent for drying, thus obtaining a finished product. The Faropenem sodium freeze-dried powder injection is simple and feasible in preparation process, beneficial to operation, and suitable for needs for large-scale industrial production.
CN103417522A Applications of L-serine in preparing medicines used for treating brain injuries and nerve tissue injuries The invention discloses applications of L-serine or medicinal salts thereof in preparing medicaments used for preventing and treating brain injuries and nerve tissue injuries. The research finds that the L-serine is capable of significantly improving the neural functional grade of a mouse with traumatic brain injuries, reducing brain tissue loss after being injured, alleviating hippocampal neuron neuronal degeneration and necrosis significantly, and improving learning and memory functions. The applications of the L-serine as a nerve protection medicine in treating acute injuries caused by the brain injuries are disclosed for the first time.
CN1732926A Medicine contained soft capsule The invention relates to a medicinal oral preparation containing anethol trithione, more specifically, the invention relates to a soft capsule for enhancing the beneficial effects of the anethol trithione.
US20130209441 Process for inhibition of cerebral damage associated with ischemia by anthocyanins and anthocyanidins A process is provided for inhibition of neural damage associated with an ischemic event that includes the administration of anthocyanin compound to a subject. After allowing sufficient time for the anthocyanin compound to reach the situs of the ischemic event, inhibition of neural damage associated with the ischemic event occurs. Neural damage is further inhibited by administration of the anthocyanin compound in conjunction with an agent effective in and specifically including tissue plasminogen activator. The anthocyanin compound in specific embodiments is in pure form or a mixture of two or more anthocyanins, or anthocyanidins or aglycones thereof, with the mixture being a natural product extract. A composition is also provided that includes ananthocyanin compound to cause blood clot dissolution. The agent being in specific embodiments is tissue plasminogen activator or aspirin.
US20120289534 Package for improved treatment of conditions The present invention provides an improved package from the administration of active ingredients. The present invention provides a package comprising: a standard portion comprising one or more active ingredients in a plurality of different potencies, and a rescue portion comprising one or more same or different active ingredients. The package may be optionally be used with a patient assessment module. The present invention also provides a kit comprising: a package comprising a standard portion comprising one or more active ingredients in a plurality of different potencies, and a patient assessment module comprising instructions for administration of the standard portion. The package may optionally further comprise a rescue portion.
EP1414408B1 Composition comprising paroxetine and a pharmaceutically acceptable glycyrrhizinate salt A taste-masked formulation of paroxetine comprises a dry blend of paroxetine and a glycyrrhyzinate, especially paroxetine hydrochloride and ammonium glycyrrhyzinate, as a dispersible powder or moulded into a dispersible or chewable tablet.
US7601724 Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. An illustrative compound of the invention is shown below:
CN101095688A Application of mannose in the preparation of medicine for treating pulmonary inflammation disease The invention provides the application of carubinose in preparing medicine that can treat lung acute inflammation diseases. The molecular formula of carubinose is C6H12O6, the structure is D-carubinose. Said medicine comprises medicine acceptable shaping agent or carrying agent. The produced dosage form mainly comprises liquid dosage form, granule, tablet, gas spraying form, drop or pill. The invention can reduce the lung tissue TNF-alpha level of mice ALT model induced by LPS, release neutral granulocyte wettability in lung tissue, inhibit capillary blood permeability, decrease protein exudation and lung water content, reduce MPO level in BALF supernatant and improve pathologic change for lung tissue inflammation. The invention discloses the functions of anti-inflammation, anti-oxidation and pneumochysis reduction of carubinose.
US8318704 Modulation of neural stem cells and neural progenitor cells The invention relates generally to methods of influencing central nervous system cells to produce progeny useful in the treatment of CNS disorders. More specifically, the invention includes methods of exposing a patient suffering from such a disorder to a reagent that modulates the proliferation, migration, differentiation and survival of central nervous system cells via S1P or LPA signaling. These methods are useful for reducing at least one symptom of the disorder.
CA2640978A1 Contraceptive composition The present invention relates to a contraceptive composition including an effective amount of a dendrimer compound including one or more naphthyl disulphonic acid surface groups, or a pharmaceutically acceptable salt or solvate of the dendrimer compound; and a pharmaceutically acceptable carrier, excipient and/or diluent therefor. The contraceptive composition may also exhibit antimicrobial activity. The invention also relates to a method of selectively reducing or preventing conception in a female animal, including a human, which method includes administering to the animal an effective amount of a contraceptive composition which composition includes an effective amount of a dendrimer compound including one or more naphthyl disulphonic acid surface groups, or a pharmaceutically acceptable salt or solvate of the dendrimer compound; and a pharmaceutically acceptable carrier, excipient and/or diluent therefor.
CN102670648A Liquid iodine disinfectant, preparation method and used container thereof The invention discloses a liquid iodine disinfectant, a preparation method and a used container thereof. The liquid iodine disinfectant comprises iodide, an oxidant capable of oxidizing the iodide to generate iodine molecules, and a pH regulator used for regulating the mixture of the iodide and the oxidant to be acidic, the disinfectant consists of a preparation I containing the iodide and a preparation II containing the oxidant and the pH regulator, and the preparation I and the preparation II are both liquid. The liquid iodine disinfectant disclosed by the invention is good in stability, can be stored for a long time, has little skin irritation, can permeate fast and volatilize quickly, does not need deiodination, and is light in coloring, excellent in sterilization effect, and safe and convenient to use and carry. The liquid iodine disinfectant disclosed by the invention has broad spectrum bactericidal action and low irritation to the skin mucosa, so that the liquid iodine disinfectant can be applied to various skin diseases caused by bacteria, funguses and viruses.
CN101830854B Substituted phenylhydrazones compounds, preparation method and application thereof The invention relates to substituted phenylhydrazones compounds, a preparation method and application thereof, in particular to novel multi-substituted single or dual phenylhydrazones compounds, a preparation method and application thereof in preparing drugs for treating singapore hemorrhagic fever and the like caused by dengue virus. A structural formula of the compounds is shown in the specification. The compounds can be used as a dengue virus NS2B-NS3 protease inhibitor, thereby preventing further proliferation of the dengue virus in a host.
WO2013021935A1 Compound for treating cartilage disorders The present invention provides a compound which can be injected into a joint cavity which is an affected part of cartilage disorders and can be accumulated in the joint cavity to exert the pharmacological effect thereof in a sustained manner, for the purpose of ameliorating cartilage disorders without developing any adverse side effect. The active form of the compound is represented by general formula (A). A compound according to the present invention, which is represented by general formula (I) (wherein all of symbols are as defined in the description), is a compound that can achieve the above-mentioned purpose. This compound does not exhibit any adverse side effect on the cardiovascular system even when the compound is administered in an effective amount for exhibiting a cartilage regeneration activity, and is therefore extremely useful as a safe and effective prophylactic and/or therapeutic agent for cartilage disorders. A suspension produced using this compound can be injected into an affected part without requiring the incision of the affected part, can therefore reduce the burden on patients, and is extremely useful as a medicinal agent.
CN1730027A Method for preparing anti-hepatitis active part from swertia main pharmaceutical plant The invention provides a method for preparing hepatitis-resisting active sites mainly from medicinal herbal Swertiamarin, which comprises: (1) disintegrating and extracting in water or water hydrophilic organic solvent through backflow, filtering to obtain merged concentration liquid, freezing, centrifugally filtrating, obtaining extract, (2) passing through macroscopic adsorption resin columns, (3) water scrubbing the resin columns, purging with 10-70% ethanol or methanol, collecting the eluent and concentrating.
WO2011058210A1 Formulations of cationic lipoamino acids with lower haemolytic power based on the formation of catanionic pairs The present invention relates to a composition consisting of a cationic surfactant, which is a diacylglycerol derived from arginine, and at least one phospholipid. The structure of said composition imparts antibacterial and antileishmaniasis properties, with reduced haemolytic power, making said composition suitable for use in the production of a drug for treating infections caused by bacteria and protozoa.
CN101205214A Benzimidazole compounds for antiphlogistic and analgesic actions The benzimidazole compounds used for anti-inflammation and analgesia provided by the invention are 2-[2-(4-morpholinyl) ethylsuleenyl]-5-(difluoromethoxy) benzimidazole (BM-2) and 2-[3-(4-morpholinyl) propylthio]-5-(difluoromethoxy) benzimidazole (BM-1), the preparation method of which comprises the following steps: the ethanol solution containing 0.01 parts by weight of 4-(3-chloroethyl or chloropropylt) morpholine is added drop by drop in the ethanol-water (2 to 1) solution containing 0.01 parts by weight of 2-mercapto-5-(difluoromethoxy) benzimidazole and 0.025 parts by weight of potassium hydroxide and the mixtures are continuously stirred and refluxed with carrying out the reaction for 6 hours after the drop-by-drop additon is finished, and then the solvents are removed through steaming by reducing the pressure; the residue is dissolved by adding water and then is extracted using the chloroform; the solvents are removed through steaming by reducing the pressure after the chloroform layer is dried through the magnesium sulfate; the residue is dissolved by being added in the ethanol and the hydrogen chloride is pumped in the obtained solution till the solution is saturated; then the saturated solution is cooled down and subject to the pumping filtration so as to obtain the crude products; then the crude products are recrystallized using the anhydrous alcohol so as to obtain the target products. The invention has the advantages of strong anti-inflammatory activity and weak gastrointestinal side effects.
EP0861329B1 Dodecahedral adenoviral protein complex, composition containing same and uses thereof A native or recombinant adenoviral protein complex, a pharmaceutical composition containing said protein complex, and the uses thereof for treating and preventing human and animal diseases, are disclosed. Said adenoviral protein complex consists of either 12 pentons each including at least one fibre and a penton base but no other element from an adenovirus genome, said fibre(s) and said penton base being derived from one or more adenoviruses, said pentons being bound by the penton bases and forming a proteolytic enzyme-stable dodecahedral structure, said complex having a molecular weight between 4.8 x 106 and 6.6 x 106, and such complexes being known as dodecahedron-penton complexes; or 12 penton bases but no other element from an adenovirus genome, said penton bases being derived from one or more adenoviruses and forming a proteolytic enzyme-stable dodecahedral structure, said complex having a molecular weight between 3.2 x 106 and 4 x 106, and such complexes being known as dodecahedron-base complexes.
EP1917015A1 Novel 4-amino-thieno[3,2-c]pyridine-7-carboxylic acid amides The present invention relates to novel 4-amino-thieno[3,2-c]pyridine-7-carboxylic acid amides of formula (I), and their pharmaceutically acceptable salts and esters which compounds of formula (I) are selective inhibitors of KDR and/or FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular solid tumors of the breast, colon, lung and prostate. Also disclosed are pharmaceutical compositions or medicaments containing these compounds, processes for making them and methods of treating cancer using these compounds.
US20100197778 Proanthocyanidins for the treatment of amyloid and alpha-synuclein diseases A method of treating an amyloid disease, or a disease characterized by IAPP amyloid fibrils or islet amyloid deposits, in a mammalian subject. The method includes administering to the mammal a therapeutically effective amount of a various disclosed procyanidins or proanthocyanidins characterized by disclosed general formulae. A pharmaceutical composition and use of the composition comprising a therapeutically effective amount of a procyanidin and a pharmaceutically acceptable excipient. The therapeutic amount of the proanthocyanidin is selected for efficacy in treating IAPP amyloid fibrils or islet amyloid deposits in a mammalian subject.
CN102342967A Thin film coated tablets containing vitamin, ginseng and zinc sulfate and preparation method thereof The invention discloses thin film coated tablets containing vitamin, ginseng and zinc sulfate. The thin film coated tablets comprise ginseng, vitamin E, pollenin, zinc sulfate, diluent, disintegrating agent, lubricant, adhesives and water-soluble thin film coating material in a weight ratio of (140-150):(25-40):(25-40):1:(110-130):(170-190):(20-30):(5-15):(15-25). The thin film coated tablets containing vitamin, ginseng and zinc sulfate have higher dissolution rate, thereby achieving the purposes of increasing the effect taking speed and improving the bioavailability.
EP1107812B1 Gelatinous body protection article having a therapeutic additive The present invention is directed to a vitamin additive such as Vitamin A, B12, C, D, E, incorporated into the thermoplastic material of a sock (12), glove (10) or like body protection article. The thermoplastic material is preferably a block copolymer such as SEBS, SEPS and SEEPS copolymer. Additionally, the thermosplastic material can include natural oils such as grape seed oil, avocado oil, jojoba oil, canola oil, ceramides and aloe.
WO2013037207A1 N-(3-pyridine formoxyl)- 3,5-dimethyl-1- amantadine or its pharmaceutical salt for treating vascular dementia The invention relates to the application of N-(3-pyridine formoxyl)- 3,5-dimethyl-1- amantadine or its pharmaceutical salt in treating vascular dementia.
CN101648924B Hydroxamic acid compound used as histone deacetylase inhibitor and application thereof The invention discloses a compound in the formula (I) or pharmaceutically acceptable salt thereof. Ar is aryl or heterocyclic group and is substituted by optional one or more of the following groups: C1-8 alkyl, C1-8 alkoxy, halogen, nitryl, C1-8 aminoalkyl, C1-8 alkyl amino group, C1-8 thio-alkyl, C1-8 halogenated alkyl, C1-8 halogenated alkoxy, C1-8 ester group, phenyl or heterocyclic group. n is an integer between 0 and 8. The drugs prepared by the compound can be used for treating solid tumors or leukemia correlating with cell differentiation or proliferation.
WO2006102674A2 Diphenylheterocycle cholesterol absorption inhibitors Various azetidinone, pyrrolidine, imidazolidine, and oxazolidine derivative are described, as are pharmaceutical compositions containing these compound and their use for preparing medicaments for the treatment of hypercholesterolemia
US20080171050 Treatment of hyperproliferative diseases with epidermal growth factor receptor antagonists A method is provided for treating a mammal with hyperproliferative disease stimulated by a ligand of epidermal growth factor receptor. The method includes administering an effective amount of an antagonist of a member of the EGF family of receptors. The method also includes administering an EGFR antagonist in combination with a chemotherapeutic agent and/or phototherapy.
CN103251642A Application of Polyflavanostilbene A in preparing medicine for treating bile duct cancer The invention discloses an application of Polyflavanostilbene A in preparing a medicine for treating bile duct cancer, belonging to the technical field of a new application of a medicine. According to in-vitro MTT anti-tumor activity evaluation, the Polyflavanostilbene A also has an obvious inhibition effect on the growth of the human bile duct cancer cell line RBE. Therefore, the Polyflavanostilbene A can be used for preparing an anti-bile duct cancer medicine, and has good prospects in development and application. The application of the Polyflavanostilbene A in preparing a medicine for treating bile duct cancer, disclosed by the invention, is disclosed for the first time, and the inhibition activity of the Polyflavanostilbene A against bile duct cancer cells is unexpectedly strong.
US8753683 Delivery of a bioactive material A solid pharmaceutical composition comprising a water-soluble bioactive material and an encapsulating material which is present in the composition in the form of continuous solid phase, and in which solid particles of the bioactive material are dispersed and encapsulated in the continuous solid phase of the encapsulating material, wherein each of the bioactive material and the encapsulating material is normally a solid at room temperature and the melting point of the encapsulating material is lower than the melting point of the bioactive material, the bioactive material being preferably a bisphosphonate, most preferably alendronate, and the encapsulating material includes an enhancer, preferably a mono- or di-glyceride, or an encapsulating surfactant, preferably a polyoxyethylene/polyoxypropylene block copolymer having surface active properties, and a process for preparing the composition in which solid particles of the bioactive material are mixed with and dispersed in the encapsulating material which is in molten (liquid) form; and cooling the molten form of the encapsulating material to form a solid pharmaceutical composition having the solid particles of the bioactive material dispersed and encapsulated in a continuous solid phase of the encapsulating material.
CN101836954A Method for preparing stable xanthophyll-oil suspension The invention provides a method for preparing stable xanthophyll-oil suspension, which comprises the following steps of: mixing xanthophyll and plant oil at a certain temperature; making the xanthophyll suspend in the plant oil in the form of micron-sized particles by using a high-pressure homogenizer; degassing the suspension under reduced pressure; packaging the degassed suspension in packages; and sealing and keeping the packaged suspension in a dark place. Under the condition that no additive is added, the stability of the xanthophyll can be greatly enhanced and the service life of the xanthophyll is more than two years under a conventional storage condition. The method is simple, convenient and suitable for industrial production.
US20090286824 Pyridine Classical Cannabinoid Compounds and Related Methods of Use Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.
WO2012023582A1 4-isopropylphenyl glucitol compound Provided is a compound for inhibiting abnormal glucose intolerance and postprandial hyperglycemia in diabetic patients by inhibiting the activity of sodium-glucose transporter 1 (SGLT 1) and the absorption of glucose. Specifically provided are a 4-isopropylphenyl glucitol compound represented by formula (I) and a pharmaceutically acceptable salt of said compound. In the formula, R1 represents a hydrogen atom or an optionally substituted C1-4 alkyl group; R2 and R3 represent a hydrogen atom, methyl group, ethyl group or a hydroxymethyl group; R4 and R5 represent a hydrogen atom, a methyl group or a hydroxymethyl group; n is 0 or 1; R6 represents a hydrogen atom, an optionally substituted piperidyl group or an optionally substituted C1-6 alkyl group; R7 represents a hydrogen atom or a C1-4 alkyl group; W represents a single bond, a methylene group or a carbonyl group; and Y represents a C1-4 alkylene group or carbonyl group.
CN101433549B Use of nano selenium in preparing calcium oxalate crystallization inhibitor The invention discloses calcium oxalate crystallization inhibitor and application thereof. The inhibitor is prepared by nano selenium which is obtained by mixed reaction of selenite solution and vitamin C solution according to certain proportion. Preferably, the selenite is sodium selenite or selenium dioxide, and the vitamin C is reduced vitamin C. The invention uses the nano selenium to preparethe calcium oxalate crystallization inhibitor for the first time; and the obtained inhibitor can effectively inhibit growth and gather of calcium oxalate, and can be used for preparing calculus inhibiting medicament of the calcium oxalate.
CN103202836A Applications of artemisine derivatives and pharmaceutically acceptable salts thereof in preparing drugs for treating acute myelocytic leukemia The invention discloses applications of artemisine derivatives and pharmaceutically acceptable salts thereof. The artemisine derivative-arteether dimer amine and the pharmaceutically acceptable salts thereof can inhibit the proliferation of leukemic cells, block the cycle of leukemic cells and induce the apoptosis of tumor cells. The artemisine derivative-arteether dimer amine and the pharmaceutical salts thereof provided by the invention can be applied in preparing drugs for treating leukemia, especially in preparing drugs for treating acute leukemia, more especially in preparing drugs for treating acute myelocytic leukemia, and particularly in preparing drugs for treating M2a subtype acute myelocytic leukemia.
CN102727895A Pharmaceutical composition for targeting treatment of intractable epilepsy The invention belongs to the biological medicine field, and relates to a pharmaceutical composition for targeting treatment of intractable epilepsy, the pharmaceutical composition of the present invention contains a micromolecule compound or a monoclonal antibody or virus vector carrying micromolecule interference RNA, the effective dosage of the micromolecule compound or the monoclonal antibody or the viral vector carrying micromolecule interference RNA in the composition on the P-glycoprotein expression inhibition efficiency can reach 30% or more than 30%, the animal experiment result shows that the effective dosage can perform the effects for inhibiting the epilepsy attack frequency and the attack duration. The corresponding brain wave presents the similar change with the epilepsy attack frequency and the attack duration.
EP2246060A1 Liver function-protecting agent Disclosed is a liver function-protecting agent which comprises a phospholipid as an active ingredient, and which can exhibit an excellent prophylactic and ameliorating effect on the deterioration in the liver function when ingested orally. Also disclosed is a liver function-protecting food, beverage or feed. The phospholipid is preferably one derived from milk or a milk material. Alternatively, the phospholipid may be used in the form of a phospholipid-containing composition prepared from milk or a milk material and containing the phospholipid in an amount of 10 wt% or more relative to the total solid content.
WO2007076379A3 4,7-dihydrothieno[2,3-b]pyridine compounds and pharmaceutical compositions This invention relates generally to compounds and pharmaceutical compositions for the treatment of myosin heavy chain (MyHC)-mediated conditions, and in particular, cardiovascular conditions.
US20120060258 Composition for use in decreasing the transmission of human pathogens A composition for coating a polypropylene-based fabric or polypropylene-based material for use in decreasing the transmission of human pathogens. A device such as a protective face mask made from a polypropylene-based fabric or polypropylene-based material coated with the composition.
CN1810242A Slow-released vincamine capsule and its prepn process The present invention provides one kind of slow-released vincamine capsule and its preparation process. The slow-released vincamine capsule contains slow-released vincamine micro pills comprising blank micro pill, active medicine layer and releasing coating. The slow-released vincamine capsule may have different micro pill combination for ideal slow-release speed for the patient to take 1-2 times a day. Compared with other vincamine preparations, the preparation of the present invention has the advantages of smooth blood medicine concentration, long maintenance time, less toxic side effect, high patient dependence in taking medicine, etc.
CN102824412A Gingiva pain-relieving, bleeding-stopping, and inflammation-eliminating composition The invention relates to a gingiva pain-relieving, bleeding-stopping, and inflammation-eliminating composition which is used after tooth extraction or when teeth are suffered from pain, bleeding, or inflammations. The composition is composed of the components of: alcohol, carbolic acid, camphor sand, clove oil, and zinc oxide, which are mixed into a paste. When in use, the composition is coated on a gingival afflicted part with a coating method, such that pain relieving, bleeding stopping, and inflammation eliminating effects can be provided. When the composition is used for preventing the teeth problems, the composition can be mixed with toothpaste, and the mixture can be used daily in tooth brushing. Or, the composition can be mixed with mouthwash, and the mixture can be used daily in mouth washing. With the composition, gingival pain can be eliminated, and gingival bleeding or inflammation can be prevented.
US8030487 2-amino—5-substituted pyrimidine inhibitors Compounds having the general structure (A) are provided. The compounds of the invention are capable of inhibiting kinases, such as members of the Src kinase family, Vegfr and various other specific receptor and non-receptor kinases.
US20120077808 Niacin Mimetics, and Methods of Use Thereof Disclosed are heterocyclylalkyl-substituted and heteroaralkyl-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.
CN102973533A Preparation method of famotidine gastric-floating-type pellet tablets The invention provides a preparation method of famotidine gastric-floating-type pellet tablets. According to the invention, gastric-floating-type pellets prepared through sustained-release coating of lightweight drug-containing pills and appropriate auxiliary materials are mixed and tableted, such that the famotidine gastric-floating-type pellet tablets are prepared. When the gastric-floating-type pellet tablets provided by the invention are orally taken, the tablets can rapidly disintegrate into independent gastric-floating-type pellets, and continuous floating and slow drug release are realized within 12h. Compared with traditional gastric-floating-type preparation, the gastric-floating-type pellet tablets provided by the invention have the characteristics of large distribution area, prolonged retention time of famotidine in stomach, and effectively improved oral bioavailability of famotidine in rat bodies. Clinically, famotidine is widely applied in treatments of diseases such as gastric and duodenal ulcers, acute gastric mucosal bleeding, gastrinoma, reflux esophagitis, and the like. The famotidine gastric-floating-type pellet tablets are a novel gastric-floating-type preparation, and have a potential to improve a treatment effect. The famotidine gastric-floating-type pellet tablets have an important clinical significance.
CN1954835A Sea-buckthorn plant preparation and its preparation method A medicine for preventing and treating diseases and nourishing human body by promoting micro-circulation and blood circulation, providing 208 bioactive substances, repairing damaged organ and tissue, decreasing fat, etc is proportionally prepared from white gourd, champignon, propolis, liquourice root, seabucklthorn fruit, zinc lactate, oligose, active composite enzymic acid, taurine and auxiliary. Its preparing process is also disclosed.
CN103251709A External medicine nose through paste for treating rhinitis and preparation method thereof The invention discloses an external medicine nose through paste for treating rhinitis and a preparation method thereof. The nose through paste comprises the following main raw materials in percentage by weight: 8.0%-9.4% of asarum, 23.2%-28% of Chinese honeylocust fruits, 8.7%-9.4% of borneol, 8.7%-9.4% menthol, 5.6%-7.2% of raw calculus bovis, 0,4%-0.45% of musk, 0.40%-0.45% of venenum bufonis powder and 37.4%-43.4% of cape jasmine. The preparation method comprises the following steps of: carefully selecting substances with impurities removed; grinding into fine powder, screening at 80-100 meshes; hermetically soaking for 72 hours by adopting 45-degree edible white spirit which is 1.5 times of the main raw materials and using a porcelain jar; and extracting juice for usage; uniformly blending into a paste by adopting medical vaseline which is 1.5 times of the main raw materials so as to prepare the nose through paste. The nose through paste disclosed by the invention is an external paste medicine used for treating the rhinitis, is used without toxic side effect or recrudescence and has the advantages of lower cost, convenience for application, simple preparation method and wide application value.
US7566709 4-(3-(2-Fluorophenyl)-1-phenyl-1H-pyrazol-4-ylmethyl)morpholine; 5HT2A/5HT2C receptors; central nervous system; schizophrenia; antidepressants; dementia; Parkinson's disease; Azheimer's disease; Huntington's disease; Tourette's syndrome; anxiolytic agents; congnition activators; analgesics Compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R5 and Q have the meanings indicated in Claim 1, are suitable as ligands of 5 HT receptors; as well as intermediate compounds of the formula (IA).
US20080085324 Compositions and methods for detecting and treating renal injury and inflammation Renal injury and inflammation is diagnosed by detecting an elevation in GSK3b level or activity. Inflammation of bodily tissues such as renal tissue is inhibited by administration of GSK3b inhibitory compositions.
CN102093261A Salicylic acid metformin salt and preparation method and medical application thereof The invention relates to the field of medicinal chemistry, in particular to a novel salicylic acid metformin salt. A salt compound can be applied to the preparation of a medicament for treating diabetes and complications of diabetes, a medicament for treating cerebral ischemia, a medicament for treating cardiovascular diseases, medicaments for treating thrombus and atherosclerosis or a medicament for treating metabolic syndrome. The invention also relates to a method for preparing the salt compound.
US20080262012 Pharmaceutical compositions comprising polymorphic forms alpha, beta, and gamma of rifaximin Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin α and rifaximin β, and a poorly crystalline form referred to as rifaximin γ, useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.
US20090042992 Polymorphs of suberoylanilide hydroxamic acid The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.
CN102600137A Application and preparation method of clonidine hydrochloride in preparation of information therapeutic drug and novel drug prepared by preparation method The invention discloses application and a preparation method of clonidine hydrochloride in preparation of an information therapeutic drug and a novel drug prepared by the preparation method. The information therapeutic drug is characterized in that the drug does not contact a human body directly during treatment, any substance ingredient of the drug can not be consumed, only drug information is utilized for physical treatment, but the chemical treatment effect can be achieved, a treatment window is enlarged by 5,000-50,000 times, and the side effects of chemical treatment are avoided. After clonidine is used as the information therapeutic drug, the contents of active ingredients are not changed, and clonidine can also be used as a conventional preparation in the chemical treatment for secondary effective use.
CN1939285A Oral preparation containing cephradine and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains cefradine. Its preparing process is also disclosed.
CN1736488A Method for preparing nanometer sized rapamycin/chitosan enveloped carrier The invention provides a method for preparing nanometer sized rapamycin/chitosan enveloped carrier, characterized in that, ionotropy technology, sol-gel technology, microemulsion technology and ultrasonic cavitation technology are employed, and comprises the steps of chitosan nano modification, rapamycin nano modification and coating to nano rapamycin by nano chitosan. The coating member has the structural features of rapamycin and chitosan.
US7066184 use of selected uncharged and cationic benzotriazole UV absorbers in the cosmetic treatment of human hair for protection against UV radiation; have affinity for hair so stays for longer periods The use of benzotriazole UV absorbers of formula (1), wherein A is a radical of formula (1a); (1b); or (1c); B is a radical of formula (1d); (1e); (1f), (1g); (1h); (1i); (1k); (1l); (1m); or (1n); R1, R2, R3, R4, R5 and R6 are each independently of the others hydrogen, C1–C16alkyl; C5–C7cycloalkyl; halogen; R9 is hydrogen, C1–C12alkyl; or C5–C7cycloalkyl; R7, R8 and R10 are each independently of the others hydrogen, C1–C12alkyl C5–C7cycloalky, C1–C12hydroxyalkyl; X is halogen; a radical of formula (1s); (1t); or (1u); sulfate, phosphate, lactate, citrate, tartrate; R11 is C1–C12alkyl; or C5–C7cycloalkyl; R12 and R13 are each independently of the other hydrogen; or C1–C5alkyl; x is from 0 to 10; and y is from 1 to 20; in the cosmetic treatment of human hair for protection against UV radiation is described.
CN1903835A Compound, composition and method for preventing neurodegeneration in acute and chronic injury of central nervous system The present invention provides a compound capable of preventing and curing nervous system diseases due to neuronal death and its method. Said invention includes synthesis of 5-benzyl aminosalicylic acid (BAS) and its derivative. The BAS and its derivative can protect cortical neuron from toxic injury of N-methyl-D-aspartate, zinc ion and active oxygen cluster, so that said invention provides compound and method for curing the diseases of apoplexy, cerebral trauma, epilepsy, spinal cord injury and neurodegenerative disease, etc.
WO2011057262A2 Treatment of infections with tp receptor antagonists The present invention relates to TP Receptor Antagonists for treatment of infection, Prodrugs and salts of the present pharmaceutical compositions are also provided.
US20120295950 Rbp4 in insulin sensitivity/resistance, diabetes, and obesity Methods for screening molecules that modulate the activity of Retinol Binding Protein 4 (RBP4) and their use in treatment of insulin resistance are described. Also described are methods of diagnosing insulin resistance and related conditions by detecting modulation of RBP4 activity.
WO2005009384A2 Egfr tyrosine kinase inhibitors The invention encompasses compounds that inhibit, modulate, or regulate kinases, compositions that contain kinase inhibiting compounds, and methods of treating kinase-dependent diseases and conditions in subjects in need of such treatment. Also, the invention encompasses methods of making compounds that inhibit, modulate or regulate kinases.
CN102558067A 1-arylsulfonyl-1H-benzimidazole derivative and preparation method and application thereof The invention relates to a 1-arylsulfonyl-1H-benzimidazole derivative and a preparation method and application thereof, belonging to the field of chemical medicine. The 1-arylsulfonyl-1H-benzimidazole derivative has a structure shown by formula I in the specification. According to the invention, the 1-arylsulfonyl-1H-benzimidazole derivative is obtained based on massive screening, and has anti-HCV activity; and a new option is provided for the development and application of a medicine for resisting chronic hepatitis C.
CN103159821A Lanostane triterpenoid and application thereof The invention discloses novel lanostane triterpenoids with two novel structures and an application of the novel lanostane triterpenoids in preparation of antitumor activity pharmaceuticals. A targeted screening result aiming at tumor specific mutant gene products shows that the two novel lanostane triterpenoids with similar structures have cytotoxic activity on tumor cells with tumor specific mutant genes p53 and Ras, and do not have or only have low cytotoxic activity on normal cells, the characteristic shows that the novel lanostane triterpenoids and therapeutically effective amounts of pharmaceutical compositions thereof have application potential on preparation of individual-based treatment pharmaceuticals for tumor specific mutant genes p53 and Ras.
US20090060983 Method And Composition For Making An Orally Disintegrating Dosage Form The present invention relates to a process for making orally disintegrating dosage forms and means for packaging such dosage forms.
US20090075966 Deuterium-enriched tazobactam The present application describes deuterium-enriched tazobactam, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN101524325B Compound menthol microemulsion and preparation for nose The invention discloses a compound menthol microemulsion and a preparation for the nose. Menthol and camphor have congruent melting performance after being mixed so as to form unctuous liquid, and an emulsifier, an auxiliary emulsifier and other additives are added to prepare transparent and stable microemulsion with the grain diameter smaller than 100 nm. The compound menthol microemulsion is used as a diluent carrier, is combined with excipient accepted by pharmacy and can be made into safe, stable and convenient nose drops and jellies for the nose so as to cure rhinitis sicca.
CN1559412A Freezing-drying powder-injection contg. sodium folinate, and its prepn. method A sodium folite injection in the form of freeze-dried powder is prepared through dissolving the freeze-drying skeleton in the water for injection, adding activated carbon, boiling filtering to remove carbon, adding folinic acid, suspending, dripping NaOH, stirring to obtain sodium folite, and mixing with the decarbonated freeze-drying skeleton, and freeze drying.
US20110319354 Combination Cancer Therapy with an AKT Inhibitor and Other Anticancer Agents The invention relates to combination anticancer therapy with certain Akt inhibitor and other anticancer agents such as anticancer antimetabolites, anticancer antibiotics, plant-derived anticancer agents, anticancer platinum-coordinated complex compounds, anticancer camptothecin derivatives and anticancer tyrosine kinase inhibitors.
WO2009039859A1 Ring-substituted phenyl pyrrole aminoguanidine derivatives The present invention relates to novel compounds of the general formula (I). The present invention further relates to the use of such compounds or pharmaceutically acceptable salts thereof for the treatment of diseases associated with the melanocortin receptors or related systems.
US20050019304 Novel human mage-like protein The present invention provides a human MAGE-like protein (MAGELP) and polynucleotides which identify and encode MAGELP. The invention also provides genetically engineered expression vectors and host cells comprising the nucleic acid sequences encoding MAGELP and a method for producing MAGELP. The invention also provides for agonists, antibodies, or antagonists specifically binding MAGELP, and their use, in the prevention and treatment of diseases associated with expression of MAGELP. Additionally, the invention provides for the use of antisense molecules to polynucleotides encoding MAGELP for the treatment of diseases associated with the expression of MAGELP. The invention also provides diagnostic assays which utilize the polynucleotide, or fragments or the complement thereof, and antibodies specifically binding MAGELP.
CN102232965A Local washing method The invention discloses a local washing method, which is to use subacid electrolyzed water which is generated by electrolysis of diluted hydrochloric acid and of which the pH value is more than 4 and less than 7 and the concentration is more than 5 ppm and less than 50 ppm for local washing or use the subacid electrolyzed water for filling a removable container. The method disclosed by the invention is low in cost, avoids local irritation and side effects and can sterilize effectively; and the used subacid electrolyzed water can be used as washing water for washing toilets.
CN101745090A Medicinal oil for treating burns and scalds and preparation method thereof The invention discloses a medicinal oil for treating burns and scalds and a preparation method thereof. The medicinal oil is prepared from the following raw materials by weight: 8 to 12 grams of corallodiscus flabellatus; 8 to 12 grams of dried ginger; 15 to 25 grams of garden burnet root; 8 to 12 grams of chicken's gizzard-membrane; 12 to 18 grams of rhubarb; 12 to 18 grams of ice stone; 5 to 8 grams of sinkiang arnebia root; 12 to 18 grams of borneol; 500 to 1,000 grams of balsam; and 45 to 55 grams of one mole. The preparation method prepares the raw materials into the medicinal oil by the steps of preparing the raw materials, stir-frying, cooling, storing and the like. The medicinal oil is not easy to be volatilized and has simple and convenient preparation process. The medicinal oil prepared by the preparation method has effect of releasing swelling, relieving pain, activating blood, dissolving stasis, removing necrosis and promoting granulation, and has obvious curative effect and quick cure time when being used for treating the burning and scalding positions.
WO2013149258A2 Compositions and methods for treating or preventing metabolic syndrome disorders The invention provides methods, compositions, uses of compositions, assays and kits for modulating brown adipose tissue (BAT) in animals and patients with obesity, insulin resistance and perturbed glucose homeostasis are disclosed. Accordingly, methods, compositions, uses of compositions, and kits are useful for the amelioration of pathological conditions characterized by storage of excess energy, insulin resistance and related metabolic syndromes often associated with obesity.
CN103301187A Secret recipe for treating rectocele The invention provides a secret recipe for treating rectocele. To achieve the purpose of the invention, the secret recipe is composed of 500 ml of snow water, 300 g of dried fruit of a locust tree and brown sugar, wherein brown sugar is used as a guiding drug, and a small amount of brown sugar is added during administration of the secret recipe. The secret recipe comprises the following preparation steps: completely soaking 300 g of the fruit of the locust tree in 500 g of snow water for 30 and 40 d and storing an obtained product in shade, wherein the longer soaking time is, the better a therapeutic effect is. It is optimal that pericarp of the fruit of the locust tree is totally dissolved during soaking and the fruit swells due to soaking, a small amount of brown sugar is added as the guiding drug into snow water after soaking, and an obtained product can be directly taken. Water obtained after soaking of the fruit of the locust tree with snow water can be used for external application. An excellent effect is obtained through combined oral administration and external application of the water; rectal mucosal prolapse of rectocele and hyperemia, edema, hemorrhage, erosion and ulcer of rectal mucosa can be thoroughly, fundamentally and rapidly treated; and a treatment rate of 98% can be obtained in treatment of rectal mucosal prolapse, full-thickness rectal prolapse and prolapse of rectums and colon sigmoideum.
WO2012008317A1 Agent for promoting energy consumption Disclosed is an agent for promoting energy consumption which comprises rice bran extract as an active component.
CN103524318A Application of allyl-containing monocarbonyl curcumin analogs in preparing antiinflammatory drugs The invention provides allyl-containing monocarbonyl curcumin analogs with antiinflammatory actions. In addition, the invention also provides a pharmaceutical composition of the compounds, antiinflammatory application and the like.
CN103330683A Tenofovir disoproxil fumarate fine granules The invention relates to tenofovir disoproxil fumarate fine granules. The tenofovir disoproxil fumarate fine granules are formed by the following steps of: mixing tenofovir and a sweetening agent according to a mass ratio of 1: (0-6); mixing the mixture with a polymer for hot melting extrusion according to a mass ratio of 1: (2-15); then carrying out hot melting extrusion through a hot melting extruder; and crushing into the fine granules with the grain diameter less than or equal to 30 meshes. The tenofovir disoproxil fumarate fine granules disclosed by the invention overcome the disadvantages that the taste of tenofovir disoproxil fumarate is very bitter and the taste masking effect of an existing preparation is not enough, and the medicine-taking compliance of a patient is greatly improved.
US20120129901 Triterpenoid derivatives useful as antiproliferative agents Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.
WO2010040232A1 Use of scyllo-inositols for the treatment of macular degeneration-related disorders The invention relates to pharmaceutical compositions comprising a scyllo- inositol of formula Ia or Ib, wherein one or more hydroxyl groups are replaced with substituents selected from the groups consisting of: alkyl, alkenyl, alkynyl, alkoxy, halogen, amino, -PO3H2, thio and sulfate. The use of these compositions in preventing or treating a macular degeneration-related disorder are also disclosed.
WO2008043740A8 Use of lansoprazole for the treatment of frequent heartburn Improvements in the treatment of patients suffering from frequent heartburn are provided by a treatment regimen comprising administration of an effective daily amount of lansoprazole or a pharmaceutically acceptable salt thereof for up to 14 days.
US7405194 Therapeutic agents and methods of use thereof for the treatment of melanoma The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.
US20090264433 Compounds, Compositions and Methods Comprising Triazine Derivatives The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
CN103340856A Rifaximin medicine composition and preparation method thereof The invention discloses a rifaximin medicine composition and a preparation method of the rifaximin medicine composition. The rifaximin medicine composition comprises the following ingredients in percentages by mass: 40-60% of rifaximin, 10-50% of microcrystalline cellulose, 1-30% of sodium carboxymethyl starch or sodium carboxymethyl starch, 0.5-6% of silicon dioxide, 0.5-6% of stearic acid and a little amount of aqueous solution of hydroxy propyl cellulose with the mass concentration of 0.5-6%. The medicine composition can be made into tablets and capsules, each dose comprises 550mg of rifaximin respectively, and a coating solution for the preparation is an aqueous solution of opadry with the mass concentration of 5-30%. The invention also provides the preparation method of the rifaximin medicine composition. According to the rifaximin medicine composition and the preparation method of the rifaximin medicine composition disclosed by the invention, the preparation of the medicine composition can be rapidly disintegrated to fully take medicine efficacy, so as to improve the health of a patient suffering from liver cirrhosis recurrent hepatic encephalopathy.
CA2315975C Phospholipid-coated microcrystals for the sustained release of pharmacologically active compounds and methods of their manufacture and use The present invention relates to pharmaceutical composi-tions for the sustained release of pharmacologically active com-pounds, and methods of their manufacture and use. The phar-maceutical compositions contain microcrystals of pharmacologically active compounds which are encapsulated within a phos-pholipid layer which contains a unique combination of phos-pholipids. The pharmaceutical compositions may be rendered suitable for injection. The microcrystals are of varying sizes. At least 50 percent of the microcrystals are from 0.5 µm and 3.0 µm in diameter, at least ten percent of the microcrystals are from 3.0 µm to 10 µm in diameter, and the composition contains microcrystals which are greater than 10 µm in diameter. The methods disclosed contain the steps of forming a lipid suspen-sion which contains the pharmacologically active compound and passing the lipid suspension with the pharmacologically active compound through a homogenizer at high pressure to coat the compound with the lipid suspension, thereby producing water insoluble drugs coated with the lipid suspension. The method is applicable to antibiotics, anti-inflammatory agents, anesthetics, anti-protozoa agents or any compound, including water soluble compounds, which can be modified so as to behave more like water insoluble compounds. The compositions and methods are useful for treating respiratory diseases in a variety of mammals. The compounds and methods are also able to sharply reduce the toxicity of drug compounds.
CN103495008A Preparation and application method of externally applied prescription for burns, scalds and bacterial festers The invention is a method of external application of an external prescription for rapidly curing ulcers caused by burns, scalds and skin bacterial infection. The externally applied prescription is prepared by the following steps: repeatedly grinding the same amount of schnittlauch, purslane and quicklime powder and evenly stirring to prepare ball pills; air-drying and micro-grinding; carrying out moisture-proof packaging on the crushed bluish white powder to obtain an externally applied Chinese patent drug prescription (quick-healing powder).
WO2009157799A1 Agent for treating and preventing oncological diseases and a method for the use of said agent (variants) The invention relates to medicine and can be used for treating and preventing oncological diseases. The inventive agent for treating and preventing oncological diseases comprises an active agent and auxiliary components. The components of the liquid agent are contained in the following amounts by weight: 1000-1100 ml lemon juice, 1000-1100 g fructose, 500-550 ml ethyl alcohol at 40 %, 35-55 g calcium chloride, 0.05-5 mg calcium chloride (calcium-41), 1-12 g zinc oxide and 0.15 mg (6000 ME) cholecalciferol (vitamin D3).
US20110021454 Modified 4`-nucleosides as antiviral agents Compounds, methods and compositions for treating a host infected with human immunodeficiency virus and hepatitis B virus comprising administering an effective amount of a described 4′-C-substituted β-D- and β-L-nucleoside or a pharmaceutically acceptable salt or prodrug thereof, are provided.
CN103040846A Medicament for resisting platelet aggregation The invention discloses a medicament for resisting platelet aggregation, and aims at solving various problems when ticlopidine hydrochloride is independently used as anti-thrombosis preparation. The medicament comprises the following components in parts by weight: 5 to 10 parts of Cu(II)2 (acetylsalicylate)4, 50 to 100 parts of ticlopidine hydrochloride, and 0.2 to 0.5 part of nitrendipine. According to the medicament, the Cu(II)2 (acetylsalicylate)4, calcium antagonist nitrendipine and ticlopidine hydrochloride which are available and low in price are combined for use; the ticlopidine hydrochloride, Cu(II)2 (acetylsalicylate)4 and calcium antagonist nitrendipine can exert synergistic action, can reduce the dosage of the ticlopidine hydrochloride, and have inhibition effect on platelet aggregation. Thus, the dose of ticlopidine hydrochloride can be greatly reduced on the premise that the curative effect of ticlopidine hydrochloride is guaranteed.
US20100136144 Composition containing a quinoa extract for dermatological use The present invention relates to a composition containing a quinoa grain extract, said extract being a peptidic and osidic extract or a lipidic extract of quinoa grain, said lipid quinoa extract being itself chosen from a group comprising an oil concentrated into its non saponificable fraction, a non saponificable, or a refined oil. The invention also relates to methods for preparing these different extracts and to dermatological or neutraceutic applications of these extracts.
CA2640376A1 Antimicrobial ceramic material comprising metal species Materials, compositions, and medical devices for the treatment or prophylaxis of microbial, including bacterial, infections, comprising at least one water-insoluble ceramic compound and at least one metal species. Methods of making such materials, compositions and medical devices.
EP1856041B1 Crystallisation and purification of glycopyrronium bromide A method for the production of crystalline glycopyrronium bromide, comprises the reaction of glycopyrronium base with methyl bromide in a solvent, in which the solvent is selected such that the diastereoisomeric ratio of the product favours the R,S and S,R diastereoisomers over the R,R, and S,S diastereoisomers, and separating the desired diastereoisomers by one or more controlled crystallisation steps. This method gives a product having a particle size of narrow distribution.
EP1562604B1 Prostaglandin compounds for the treatment of obesity Provided is a composition for treating obesity which comprises an effective amount of a prostaglandin compound, especially, a compound of formula (I).
WO2014058078A1 Process for producing dihydro-2h-pyran derivatives Disclosed is a process for preparing dihydro-2H-pyran derivatives of formula I: wherein R1 and R2 are defined herein. The process of the invention provides the compound of formula I in concise cascade reactions and in one pot. The compound of formulae I prepared by the process of the invention and its further transformed derivatives are useful for making pharmaceutical composition for the treatment of proliferative diseases.
CA2592543A1 Use of selected compounds for protection of neurones and oligodendrocytes in the treatment of multiple sclerosis Certain compounds, including 5,6-dihydro-3,9-dihydroxyindolo[2,1-a-isoquinolin12yl)[4-[2~-(1-piperidinyl) ethoxy]phenyl]- methanone and arzoxifen, are useful for providing protection to oligodendrocytes and neurons of multiple sclerosis patients.
WO2012003563A4 Antineoplastic pharmaceutical compositions containing substituted nitroaromatic compounds The present invention describes antineoplastic pharmaceutical compositions comprising substituted nitroaromatic compounds. The compositions can be used for treating early-stage neoplasias or in combination with other antitumour drugs for more advanced stages of the disease.
EP1560588A2 Treatment for traumatic synovitis and damaged articular cartilage The invention provides compositions useful for the treatment and/or prevention of damage to diarthrodial (synovial) joints and, in particular, traumatic synovitis, inflammation of the synovial membrane, and damage to the articular cartilage of the joint. Specifically, provided are compositions specially formulated for intra-articular and/or parenteral use in the treatment and/or prevention of traumaticsynovitis and/or damage to articular cartilage. Compositions adapted specifically for post surgical joint lavage or treatment and/or prevention of inflammatory arthritis, osteoarthritis (OA) and/or degenerative joint disease (DJD) are also provided. Compositions adapted for intra-articular and/or systemic administration comprised of therapeutic amounts of: chondroitin sulfate; N-acetyl D-glucosamine; andhyaluronan (hyaluronic acid) are provided.
US20070202134 Muc1 Antagonist Enhancement of Death Receptor Ligand-Induced Apoptosis The present invention relates to methods of enhancing death receptor-induced apoptosis in MUC1 expressing cells comprising contacting the MUC1 expressing cells with an effective amount of a MUC1 antagonist.
EP1523471B1 Urea-substituted and urethane-substituted acylureas, methods for the production thereof and their use as medicaments The invention relates to urea-substituted and urethane-substituted acylureas, to physiologically compatible salts thereof and to their physiologically functional derivatives. The invention thus relates to compounds of formula (I), wherein the radicals have the cited meanings. The invention also relates to the physiologically compatible salts of these compounds and to methods for the production thereof. The inventive compounds are suited for use, for example, as antidiabetics.
EP1233748B1 Retinaldehyde combination with antifungal activity The invention concerns a cosmetic composition containing a combination of retinaldehydes and of at least a linear aldehyde comprising 6 to 12 carbon atoms, for use as cosmetic composition or medicine, its preparation method and its use for antifungal, antimicrobial treatment, in particular for treating Malassezia and for treating dry and/or greasy dandruff.
WO2009153536A1 1-aza-bicyclo [2.2.2] octane derivatives useful as muscarinic receptor antagonists The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in therapy.
CN101422438A Composite diisopropyiarmini dichloroacetas freeze-dry preparation without adjuvant and preparation technique thereof The invention relates to a diisopropylamine dichloroacetate lyophilized preparation without accessories, and a preparation method; the preparation only contains diisopropylamine dichloroacetate and sodium gluconate, and contains no additives. The lyophilized preparation of one dosage contains 2mg to 200mg of the diisopropylamine dichloroacetate and 1.9mg to 190mg of the sodium gluconat. The proportion between the medicament and water in the preparation technique is 1 : 1 to 100; a medicine liquid is prepared first; and then a pre-freezing lyophilization technique is adopted for one or a plurality of times to carry out the preparation. The invention leads the quality of the preparation to be more easily controlled, reduces the production cost and leads the medicament use safety of a patient to be ensured more. The invention can obtain excellent effects in curing clinic liver diseases.
WO2006081985A1 Combined treatment with an n4-(substituted-oxycarbonyl)-5’-deoxy-5-fluorocytidine derivative and an epidermal growth factor receptor kinase inhibitor The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGER kinase inhibitor and an N4-(substituted- oxycarbonyl)-5'-deoxy-5-fluorocytidine combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase inhibitor and an N4-(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine combination in combination with a pharmaceutically acceptable carrier. A preferred embodiment of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlotinib HCl (also known as Tarceva™). A preferred embodiment of an N4-(substituted- oxycarbonyl)-5'-deoxy-5-fluorocytidine that can be used in practicing this invention is the compound capecitabine (also known as Xeloda™).
EP2295058A1 Depot formulations of iloperidone with a polymer A depot formulation comprises iloperidone and a biodegradable, biocompatible polymer, wherein the polymer is is selected from the group consisting of polyesters
CN102499928A Pharmaceutical formulation comprising an antibiotic, a triazole and a corticosteroid Disclosed are novel formulations for the treatment of otic infections in an animal comprising a triazole anti-fungal compound, a quinolone antibiotic and a corticosteroid such as mometasone furoate monohydrate.
WO2014101765A1 Benzoxazine oxazolidinone compound, preparation method and application thereof Disclosed are a benzoxazine oxazolidinone compound shown by a general formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, a preparation method thereof, and an application thereof in preparing a drug for treating an infectious disease and in particular, an infectious disease caused by multidrug resistant bacteria.
US20100129465 Methods and Compositions Related to Acne Treatment Disclosed herein are methods and compositions for treating acne using a composition comprising a large amount of naturally occurring minerals.
WO2007004510A1 Pharmaceutical for use in the treatment of cerebral infarction Disclosed is a pharmaceutical which has an excellent therapeutic effect on cerebral infarction and an excellent ameliorating effect on a dysfunction or neurologic deficit induced by cerebral infarction and produces little adverse side effects. A pharmaceutical comprising a combination of N-(3-chloro-4-morpholin-4-yl)phenyl-N’- hydroxyimidoformamide with a thrombolytic agent such as urokinase, alteplase, desmoteplase, tisokinase, nasaruplase, nateplase, pamiteplase, monteplase or batroxobin.
CN103070870A Application of carbenoxolone in preparing anti-dengue virus medicine The invention discloses a new application of carbenoxolone, pharmaceutically acceptable derivatives thereof or medicine compositions containing either in the pharmaceutical manufacturing field. According to the experiments, the carbenoxolone can protect susceptible cells from infection by the dengue virus, which demonstrates that the carbenoxolone has underlying application value in the field of curing dengue virus infectious diseases. According to the invention, experiment evidences are provided for clinically using the carbenoxolone to cure the dengue virus infectious diseases, which has a certain guiding significance for developing anti-dengue virus medicines and also has an important reference value.
WO2010027770A1 Crystalline forms of sufentanil citrate The present invention provides crystalline forms of sufentanil citrate and methods for preparing crystalline forms of sufentanil citrate.
CN102038666A Medicament for treating or preventing metabolic diseases and application thereof The invention relates to application of 12 compounds such as LG13 shown below in the preparation of medicaments for preventing or treating metabolic diseases such as diabetes. In addition, the invention also relates to a medicinal composition containing the compound LG 13 and a medicament case. The number is LG 13.
CN102040627A Phosphorus-containing compound and its medicament application for treatment of bone metabolism abnormity The invention relates to phosphorus-containing compound and its medicament application for treatment of bone metabolism abnormity. Compared with bisphosphonates of existing structures, the compound in the invention can decrease oxidative metabolism, and increase the effective bioavailability. In addition, applying the compound for treatment of bone metabolism abnormity, can reduce the dosage and side effects. The phosphorus-containing compound in the invention is especially suitable for the treatment of hypercalcemia diseases.
WO2012068441A3 Intedanib salts and solid state forms thereof The present invention provides salts of Intedanib, crystalline forms of the salts of Intedanib, processes for their manufacture and their use in pharmaceutical compositions.
CN101134601A Novel water-soluble platinum (ó ) small molecule anticancer complex The present invention relates to one kind of small molecular platinum complex cis-[ammonia. hydroxyamine. dichloride. platinum(II)], which is prepared with K[Pt(NH3)Cl3] as initial material, and through reaction with NH2OH in water solution to obtain coarse product and re-crystallization in 1 to 1 water and methanol system to obtain refined product. The complex has high anticancer activity, high water solubility and high stability, and may find its application in treating cancer clinically.
US7208594 mixture with polysorbate; beverages, cosmetics, nutrient adjuvants, cleaning compounds, Isoflavone concentrates are described, which contain at least about ten to about twenty weight parts of polysorbate to one weight part of isoflavone containing a genistein, and/or daidcein, and/or glycitein. Further, a method for the production of an isoflavone concentrate is described.
CN102030810A Gallic acid tea sapogenol ester as well as preparation method and application thereof The invention discloses a gallic acid tea sapogenol ester as well as a preparation method and application thereof. The gallic acid tea sapogenol ester has a structure shown in the formula I and is prepared by the following steps of: reacting benzyl bromide and gallic acid to connect benzyl groups to carboxyl groups of the gallic acid and protect the carboxyl groups of the gallic acid; then, adding tea sapogenins for performing esterification with the gallic acid in the presence of a catalyst A; and finally adding a benzyl deprotection agent for removing the benzyl groups from the gallic acid in the presence of a catalyst B to obtain the gallic acid tea sapogenol ester shown in the formula I. The preparation method of the gallic acid tea sapogenol ester is simple and convenient for industrialized production, and the prepared gallic acid tea sapogenol ester has little toxicity and higher antioxidation and radical removing performances and overcomes the defect of low antioxidation activity of tea saponins.
EP2687513A1 Drugs for inhibiting aggregation of proteins invoved in diseases linked to protein aggregation and/or neurodegenerative diseases The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed.
US20120225108 Products for improving wound healing Morpholino compounds of Formula (I) wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, or pharmaceutically acceptable salts thereof, have been found to be surprisingly effective at promoting the healing of a wound.
CN1871238A Triaza-spiropiperidine derivatives for use as GLYT-1 inhibitors in the treatment of neurological and neuropsychiatric disorders The invention relates to compounds of the general formula (I), wherein A-A is -CH2-CH2-, -CH2-CH2-CH2-, -CH2-0- or -0-CH2-; x is hydrogen or hydroxy; R<1> is aryl or heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or trifluoromethyl; R<2> is aryl or heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or trifluoromethyl, or is lower alkyl, -(CH2)n-cycloalkyl, -(CH2)n-CF3, -(CH2)p-0-lower alkyl, -(CH2)1,2-phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy or trifluoromethyl, or is -(CH2)p-NRR', wherein W and R' form together with the N-atom a heterocyclic ring, selected from the group consisting of piperidine, morpholine, thiomorpholine or 1, I-dioxo thiomorpholine; R<3>, R<4> are independently from each other hydrogen, lower alkyl, phenyl or benzyl; R<5> is hydrogen, lower alkyl or benzyl; R<6> is hydrogen or lower alkyl; n is 0, 1 or 2; and p is 2 or 3; and to pharmaceutically acceptable acid addition salts thereof for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
US20080119421 producing a synchronized cells by administering a cell cycle arresting drug, then adding a microtubule stabilizing drug, and applying mechanical vibrational energy ultrasound; drug deliverying anticarcinogenic agent directed to be more toxic to cancer cells than normal cells A process for treating a biological organism, comprising the steps in which a cell cycle arresting drug is administered to the organism to produce synchronized cells, the microtubules within the synchronized cells are stabilized by means of a microtubule stabilizing agent, and the synchronized cells with the stabilized microtubules are then contacted with mechanical vibrational energy.
US20110262457 Modulation of the immune response Methods for increasing the generation of IL-17-producing T cells (TH17) in vivo and in vitro, and enriched populations of TH17 cells for the treatment of diseases benefiting from an induced or enhanced immune response, e.g., infection and cancer.
CN103140211A Skin care compositions comprising substituted monoamines Skin care compositions comprising certain substituted monoamines, which are particularly beneficial for skin lightening and achieving evenness of color, especially for face and underarm skin. The compositions contains 0.001-20% of substituted monamine with a structure I: where in R1 represents cyclohexyl, phenyl, mono- and di-substituted phenyl substituted with a moiety selected from the group consisting of: C1-C5 alkyl, C1-C5 alkoxy, phenoxy; and R2 represents hydrogen or methyl.
EP2338448A2 Anti-inflammatory and antimicrobial uses for bioactive glass A composition comprising non-interlinked particles of bioactive glass in a carrier for use in a therapeutic method selected from: accelerated healing of wounds and burns and/or for improving the appearance of scar tissue resulting from such wounds and burns; treating wounds and burns; grafting skin, reducing the level of inflammation in a wound; and reducing the level of bacterial infection in a wound.
WO2010150837A1 Indoline derivative A therapeutic agent for hyperparathyroidism, secondary hyperparathyroidism, primary hyperparathyroidism, renal osteodystrophy, hypercalcemia or the like, which has a calcium sensing receptor activation activity and comprises a compound represented by general formula (I) [wherein R1 and R2 independently represent a hydrogen atom, a halogeno group, or the like; R3 and R4 independently represent a C1-C3 alkyl group; R5 represents a hydrogen atom, or the like; R6 represents a carboxyphenyl group, or the like; and R8, R9 and R10 independently represent a hydrogen atom, a halogeno group, a cyano group, or the like] or a pharmacologically acceptable salt thereof as an active ingredient.
US20060189665 Oxamide derivatives useful as raf-kinase inhibitors The present invention relates to oxamide derivatives of Formula (I), the use of the compounds of Formula (I) as inhibitors of raf-kinase, the use of the compounds of Formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
US20090029940 Plymorphic form of inulin and uses thereof The present invention relates to a new polymorphic form of inulin, designated delta inulin (dIN), to methods for the preparation of dIN, compositions comprising dIN and uses thereof. The present invention also relates to the use of dIN and compositions comprising dIN in the preparation of gamma inulin (gIN), compositions comprising gIN and uses thereof.
EP0994710B2 Pharmaceutical compositions for oral administration, comprising a benzhydrylpiperazine and a cyclodextrin The invention concerns pharmaceutical compositions for oral administration, comprising an active substance belonging to the family of substituted benzhydrylpiperazines and at least a cyclodextrin.
US20110189270 Differential Loading Of Drug-Eluting Medical Devices A medical device includes a substrate having at least one surface. The surface has a central portion and a peripheral portion. At least one bioactive agent is disposed over at least a portion of the surface. The medical device having a concentration gradient of the at least one bioactive between the central and peripheral portions.
EP2610263A1 Sialic acid dimers Sialic acid derivatives (I) are new. Sialic acid derivatives of formula (I) or their salts, metabolites or prodrugs are new. A1, A2 : D1-[Y3-D2] m-; D1, D2 : mono- or polycyclic and aromatic, partially unsaturated or saturated 3-14C hydrocarbyl or aromatic, partially unsaturated or saturated 3-8-membered heterocyclyl (both optionally mono- or polysubstituted by X1); X1 : halo, CN, NO 2, OH, mercapto, NH 2, carboxy, hydroxylamino, azido, B(OH) 2, SO, SO 3M, OSO 3M, SO 2NH 2, SO 2CF 3, PO 3M, OPO 3M, cyanomethyl, 1-8C (halo)alkyl, 2-8C alkenyl, 2-8C alkynyl, (halo)alkyloxy, 2-8C alkenyloxy, 2-8C alkynyloxy, alkylthio, alkylamino, dialkylamino, trialkyl-amino, formyl, alkylcarbonyl, alkylsulfonyl, alkyl-sulfoxy, alkylamino-sulfoxy, dialkylamino-sulfoxy, alkyloxycarbonyl, alkylcarbonyloxy, aminocarbonyl, aminothiocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, dialkylaminocarbonyl, alkylamino-thiocarbonyl, =O, =S, 1-8C alkyl-imino or 1-8C alkyl-oximino; either Y1, Y2 : 1-4C (halo)alkyl, 1-4C alkyl-CO, -C(O)-, -CH 2-C(O)-, -CH=CH-C(O)-, -CC-C(O)-, -S(O) 2-, -CH 2-S(O) 2-, -NR11-C(O)-, -CH(CF 3)-, -NR11-3-cyclobutene-1,2-dione-4-yl, -CH 2-NR11-3-cyclobutene-1,2-dione-4-yl, -NR11-3,2,5-thiadiazole-1-oxide-4-yl or -NR11-3,2,5-thiadiazole-1,1-dioxide-4-yl; or Y1+N to which it is bonded+R8, Y2+N to which it is bonded+R8 : 1H-(1,2,3)triazol-1-yl (which is bonded to A in 4th position), 1H-(1,2,3)triazol-1-yl- (which is bonded to A in 5th position), -CH 2-1H-(1,2,3)triazol-1-yl (which is bonded to CH 2 in 4th position) or -CH 2-5-1H-(1,2,3)triazol-1-yl (which is bonded to CH 2 in 5th position); Y3 : bond, O, S, S(O), S(O) 2, CH 2, C(O), C(R11) 2 or NR11; m : 0-2; Z1 : O, S, CH 2 or NR11; D11 : Z2-T1-Y4-A3-Y5-T2-Z2; Z2 : -O-, -S-, -NR11-, -NH-C(O)-, -CH 2-, -CF 2-, -CH(OH)-, -N(R11)-O-, -O-NR11-, -O-N=CH-, 1H-(1,2,3)triazol-1-yl (which is bonded to T1 or T2 in 4th position) or 1H-(1,2,3)triazol-1-yl (5) (which is bonded to T1 or T2 in 5th position); T1, T2 : 1-30C alkanediyl (in which at least one non-terminal -CH 2- is optionally replaced by -O-, -S-, -S(O)-, -S(O) 2-, -S +>(CH 3)-, -P(O 2)- or -NR11-, at least one H is optionally replaced by F, Cl, OR11, OSO 3M, =O, =S, carboxy, NH 2, NHR12 or NHR13, at least one non-terminal -CH 2-CH2- is optionally replaced by 1H-(1,2,3)triazol-1-yl (which is bonded with remaining part of molecule in 5th position) or -CR11=CR11- or -CC-, -CH 2CH 2CH 2 is optionally replaced by 1H-(1,2,3)triazol-1-yl (yl (which is bonded with remaining part of molecule in 4th position) or -O-N=CH, and -CH 2CH 2CH 2CH 2- is optionally replaced by phenyl-1,4-diyl); Y4, Y5 : bond, O, S, NR11, S(O), S(O) 2, -C(O)-, -C(O)-NR11-, -NR11-C(O)-, -C(O)-O-, -O-C(O)-, -NR11-CO-NR11-, -NR11-S(O) 2-, -S(O) 2-NR11-, -CH 2-NR11-C(O)-, -CH 2-C(O)-NR11, -CH 2-NR11-, -CH(CF 3)-NR11, -CH=N-O- or -O-N=CH-; A3 : 1-8C alkanediyl, 2-8C alkenediyl, 2-8C alkynediyl or 4-8C alkadiene-diyl (in all groups several -CH 2- are replaced by O, S, S(O), S(O) 2, NR11 or C(O), and at least one H is optionally replaced by X2), A4-[Z3-A5] n, 1,1'-ferrocene-diyl, 1,1'-cobaltocendiyl, 1,1'-ruthenocene or diamino-dichloroplatinum-diyl; A4, A5 : saturated, partially unsaturated or aromatic 3-14C mono- or polycyclic hydrocarbyl or aromatic, partially unsaturated or saturated and mono-or polycyclic 3-8-membered heterocyclyl (both optionally substituted by X2); Z3 : bond, O, S, S(O), S(O) 2, NR11, C(O) or C(R11) 2; X2 : 1-4C (halo)alkyl or (halo)alkyloxy (both containing F or Cl), F, Cl, Br, NO 2, hydroxylamino, B(OH) 2, SO 3M, OSO 3M, SO 2NH 2, PO 3M, OPO 3M, alkylthio, alkylamino, dialkylamino, trialkyl-amino, alkylcarbonyl, alkylsulfonyl, alkyl-sulfoxy, alkylamino-sulfoxy, dialkylamino-sulfoxy, alkoxycarbonyl, alkylcarbonyloxy, aminocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, dialkylaminocarbonyl, alkylamino-thiocarbonyl, 1-4C alkyl-imino or 1-4C alkyl-oxyimino; n : 0 or 1; R1 : C(O)OM, O-PO 3(M) 2, O-SO 3M, SO 3M, C(O)-NH-S(O) 2-R11, PO 3(M) 2 or C(O)NOM; R2, R3 : H or F; R4, R7 : H, OH, OR13, OC(O)NHR12 or NR11; R6 : H or R13; R5 : H, R11, (R11) 2, C(O)H, C(O)CH 2OH or C(O)-haloalkyl; R8 : R11; M : H, 1-6C alkyl or cation; R11 : H, R12 or R13; R12 : 1-6C alkyl, phenyl or benzyl; and R13 : -C(O)-1-6C alkyl, -C(O)-phenyl or -C(O)-1-4C alkylphenyl. [Image] ACTIVITY : Antibacterial; Virucide; Antiparasitic; Immunomodulator. MECHANISM OF ACTION : None given.
CA2299630C Compositions that specifically bind to colorectal cancer cells and methods of using the same A unique transcription product, CRCA-1, and alternative translation products generated therefrom, are disclosed. The transcript and its translation products are markers for colorectal cells. Screening and diagnostic reagents, kits and methods for metastasized colorectal cancer are disclosed as are reagents, kits and methods for identifying adenocarcinomas as colorectal in origin. Compounds, compositions and methods of treating patients with metastasized colorectal cancer and for imaging metastasized colorectal tumors in vivo are disclosed. Compositions and methods for delivering active compounds such as gene therapeutics and antisense compounds to colorectal cells are disclosed. Vaccines compositions and methods of for treating and preventing metastasized colorectal cancer are disclosed.
EP2170259A1 Slimming composition This invention relates to the use of a preparation comprising sulfated oligosaccharides which trap spermine and/or spermidine, as an active slimming ingredient in a cosmetic, pharmaceutical and/or nutraceutical composition. One aspect of the invention is to supply a cosmetic, pharmaceutical or nutriceutical composition with a slimming effect.
WO2013088257A1 Substituted heterocyclic compounds as tropomyosin receptor kinase a (trka) inhibitors The present application relates to a series of substituted pyrazolo[l,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
WO2008076964A1 Therapeutics for cancer using 3-bromopyruvate and other selective inhibitors of atp production The present invention relates to methods of treating a cancerous tumor in a subject comprising administering to the subject an effective amount of 3-bromopyruvate. The 3- bromopyruvate may be administered intraarterially directly to a tumor as a continous intraarterial infusion. The present invention also relates to methods for identifying agents that inhibit type II hexokinase activity.
CN101897876A Leak disease removing paste The invention discloses a preparation method of a leak disease removing paste, which is realized by adopting the following technical scheme of: cleaning welsh-onion stalks and roots and adding hay meal; freezing for 4 hours at the temperature of -5 DEG C; taking out and then mashing with a stone mortar; then adding earthworms and white sugar and smashing for 5 min and then evenly stirring to obtain the finished paste. The disease is removed in three days by utilizing the method.
WO2012161622A3 Incretin hormone secretion stimulators, method for producing and using same The invention relates to the field of medicinal chemistry, pharmacology and medicine and contains a description of pharmaceutical compositions and combination drugs based on secretion stimulators and protectors of incretin hormones for the treatment of metabolic diseases (including diabetes, obesity, metabolic syndrome, etc.). The essence of the invention is that the pharmaceutical composition or combination drug contains a tetrahydrobenzo[f][1,4]oxazepine derivative which is a non-steroidal agonist of TGR5 bile acid receptors, or one of the endogenous bile acids, which stimulate the secretion of incretin hormones, as well as one of the known DPP-IV protease inhibitors. The TGR5 agonists are administered orally; the endogenous bile acids are administered rectally in the form of a suppository or gel. The following may be used as DPP-IV protease inhibitors: Vildagliptin, Saxagliptin, Sitagliptin, Teneligliptin, Linagliptin, Dutogliptin, Alogliptin, Gemigliptin, Carmegliptin, etc. In addition, the invention contains a description of novel derivatives of tetrahydrobenzo[f][1,4]oxazepine which are non-steroidal agonists of TGR5 bile acid receptors, as well as methods for the production thereof. The invention provides more effective therapy as a result of the synergistic action of the components, wherein it is possible to treat diabetes, obesity and other metabolic diseases and the cardiovascular and renal complications thereof simultaneously.
CN101278926B Applications of iron chelator in preparation of medicament for preventing or curing hemorrhagic cerebrovascular disease and chronic hydrocephalus after craniocerebral injury The invention discloses an application of an iron ion chelant in a preparation of a drug for preventing or treating hemorrhagic cerebrovascular disease and chronic hydrocephalus after craniocerebral injury; an animal experimental research shows that the iron ion has something to do with the emergence of the chronic hydrocephalus after ventricular hemorrhage; the iron ion chelant is capable of eliminating excessively accumulated iron ion in cerebrospinal fluid (CSF), lightening brain tissue damage caused by the iron ion, effectively reducing the incidence rate of ventricular hemorrhage hydrocephalus of a big mouse, improving the learning memory abilities of the big mouse with the ventricular hemorrhage, thereby being used for preparing the drug for preventing or treating the hemorrhagic cerebrovascular disease and the chronic hydrocephalus after the craniocerebral injury.
WO2006108127A3 Crystalline form of a quinolinone-carboxamide compound The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5 HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
CN102525934A Preparation process of cefepime hydrochloride for injecting The invention provides a preparation process of cefepime hydrochloride for injecting. The preparation process comprises the following steps of: (1) cleaning and sterilizing an amoxicillin bottle, a butyl rubber plug and an aluminum plastic cover; and (2) performing split charging.
US20080119429 Methods and means for increasing resistance to cell damage Methods are provided to increase resistance to cell damage in a subject. The increase in resistance to cell damage in a subject in the subject is accomplished by decreasing activity of eEF2 kinase in the subject. The eEF2 kinase activity can be decreased by decreasing the amount of functional eEF2 kinase produced by the subject, including contacting the eEF2 kinase with a compound that inhibits phosphorylation of eEF2 kinase substrate or decreasing the amount of functional eEF2 kinase is decreased by reducing expression of a gene encoding the eEF2 kinase.
EP1149105B1 4,5-pyrazinoxindoles as protein kinase inhibitors 4,5-pyrazinoxindoles having formula (I), inhibit or modulate protein kinases, in particular JNK protein kinases and are useful as anti-inflammatory agents, particularly in the treatment of rheumatoid arthritis.
CA2335363C Adhesively applied external nasal strips and dilators containing medications and fragrances Nasal dilators and strips, methods of their manufacture, and methods for improving the breathing of individuals are provided. The strips and dilators include an elongated substrate, with or without a dilating component or portion, having top and bottom surfaces and a pressure-sensitive adhesive disposed on the bottom surface. The dilator (100) is designed to provide a gentle expanding force to the nasal wall tissue when the dilator (100) is adhesively attached to the nose. This invention further includes a cosmetic fragrance, an aromatic medication and/or transdermal medication disposed on the strips or dilators. In order to improve the shelf-life and in-use olfactory effectiveness of such products, fragrance delivery mechanisms are used. Separation of volatile oils and adhesives are also provided to minimize adhesive residue.
WO2013010140A2 Methods of diagnosing cancer Provided are methods of predicting or assessing the level of severity of cancer or cancer progression in a patient comprising measuring levels of SET expression in a biological sample from a patient and comparing levels of SET expression to a control sample or standard value. Methods for predicting or evaluating the efficacy of a SET therapeutic and kits comprising at least one reagent for measuring SET protein expression are also provided.
US7557183 Polyethylene glycol linked GLP-1 compounds The invention provides GLP-1 compounds coupled to at least one polyethylene glycol molecule or derivative thereof, resulting in a biologically active peptide with an extended half-life and a slower clearance when compared to that of unPEGylated peptide. These PEGylated GLP-1 compounds and compositions are useful in treating diabetes, obesity, irritable bowel syndrome and other conditions that would be benefited by lowering plasma glucose, inhibiting gastric and/or intestinal motility and inhibiting gastric and/or intestinal emptying, or inhibiting food intake.
WO2003099762A8 Agents and methods for the treatment of disorders associated with oxidative stress The invention provides a method for preventing or reducing the effects of oxidative stress on a substrate. The method includes the step of treating the substrate with a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein: R1 is one or more substituents selected from -H, -alkyl, -alkoxy, -aryl, -aryloxy, -halogen, -amino (mono-, di- and tri-substituted), -alkylthio, -NO2, -COOH, -COOAlkyl, -CO-alkyl, -CN; R2 is one or more substituents selected from -H, -alkyl, -(CH2CH2O)n-R5, a sugar moiety; R3 is -H, -alkyl, -aryl, -alkylOR6 , -alkylC(O)R6; R5 is selected from -H, -alkyl, -aryl; and R4 and R6 are independently selected from -OH, -O-alkyl, -O-polyalkyleneoxy, -O-aryl, -OC(O)O-alkyl, -S-alkyl and -amino.
WO2009114088A2 Fullerene therapies for inflammation Described herein are methods for treating inflammatory disorders. The methods comprise administering to a subject in need thereof a therapeutically effective amount of a synthetically modified fullerene.
US20110263669 Novel Pyrrolo [2,3-A] Carbazoles and Use Thereof as PIM Kinase Inhibitors The invention relates to pyrrolo[2,3-a]carbazole derivatives, to a method for preparing the same, and to the use thereof as PIM kinase inhibitors. The invention can particularly be used in the pharmaceutical field.
US20120004210 Substituted quinazoline compounds The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted quinazoline compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder, In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like.
US20110229533 Extended release dosage form A membrane system comprising an interior wall, a fluid-permeable exterior wall surrounding the interior wall and an internal compartment defined by the membrane system, wherein fluid permeability of the interior wall is responsive to osmolarity of an osmotic core within the internal compartment are disclosed. A controlled release dosage form comprising the membrane system and a process for delivering an osmotically active formulation from an osmotic pump over an extended period of time are also disclosed.
WO2010038688A1 Particulate pharmaceutical composition for oral administration of atorvastatin A particulate pharmaceutical composition for oral administration, which contains (1) atorvastatin or a pharmaceutically acceptable salt thereof, (2) a surfactant selected from the group consisting of sodium lauryl sulfate and polyoxyethylene-cured castor oils, and (3) a water-soluble polymer material.
WO2004075775A3 Treatment of excessive osteolyisis with indolinone compounds Compounds of Formula I and Formula II, as described herein, are useful for treating excessive osteolysis, by inhibiting M-CSF mediated osteoclast development. The compounds also are useful for inhibiting phosphorylation of CSF1R, and for treating cancers that express CSF1R.
CN1631895A Preparation method of amygdalin and its application in preparation of amygdalin preparation for promoting the blood circulation of heart, brain, pancreas and wound Disclosed are a method for preparing amygdalin and its application in promoting blood circulation of brain and pancreas and hurt, which belong to medical application of medicine containing organic effective components. The invention has supplied a medical application of prevention, which can prevention and cure cerebral ischemia caused by increase of blood consistency, has protective effect to heart breakdown, cure acute pancreatitis, increases microcirculation of blood in skin issue and promote wound healing. Besides, a method to prepare amygdalin is disclosed, in which apricot is processed through squeezing of oil and hydrophilic degreasing by diethyl ether and other techniques, finally acquiring pure amygdalin with high productivity, purity, simple abstraction and separation.
US20100249035 Peptides, compositions and uses thereof Described is an N-terminal hexapeptide fragment of maximakinin, QUB 698.8, which exhibits potent tissue selective actions on smooth muscle. It demonstrates a high degree of selectivity for arterial smooth muscle over small intestinal smooth muscle, causing potent relaxation of arterial smooth muscle, while causing less potent contraction of ileal smooth muscle. It may be used treatment of diseases of the cardiovascular system and in promotion of angiogenesis.
US20070117820 1-([3-Chloro-5-trifluoromethylpyridinyl-2-yl]piperidin-4-yl)-3-(1-methyl-isoquinolin--5-yl)-urea hydrochloride; capsaicin receptor antagonist; calcium level blocker; lower fluorescence; neuropathic, postrheumatoid, osteoarthritic, back, cancer pain, neuralgia, migraine, neuropathies, diabetic neuropathy Compounds of formula (I): or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein: P, P′, R1, R2, n, p, q, r, and s are as defined in the specification, processes for preparing such compounds, pharmaceutical compositions comprising such compounds and their use in therapy.
CN1943685A A giantarum fat-reducing granule containing oligo polyflavanol and preparation method and use It is a kind of giantarum fat-reducing granule containing oligo polyflavanol and preparation method. The main point is: the giantarum glycn glucomannan gel granule envelopes oligo flavanol, vitamin E and mineral matters. Its preparing method:put the above raw materials according to the given ratio into the mixer to mix them , and slowly add distilled water 3-30 times by mass of the giantarum glycn glucomannan and stir them until they form into uniformed gelatin, dry the gelatin by reducing pressure in low temperature, then crush and screen them to be 0.1-2mm diameter of fine granules. These can be used as fat-reducing food. The advantage of this invention is that not only the giantarum glycn glucomannan has the fat-reducing effect, but also improved the biologic usage of the oligo flavanol, so to strengtheed the effects of fat-reduction.
CN101259138A Anti-inflammation and ease-pain composition topical application for animal kinematic scheme part The invention relates to an anti-inflammatory and pain-killing composition that can be partially used; the composition consists of the following ingredients by weight percentage: about 0.01-3 percent of hyaluronic acid, about 0.5-7 percent of extract of arnica glycol, about 2-10 percent of any hydrogel soluble non-steroidal anti-inflammatory agent, and about 70-95 percent of hydrogel.
EP1621190A1 Deprenyl compounds for treating Multiple Sclerosis A method for increasing the survival of oligodendrocytes, comprising administering an effective amount of a deprenyl compound to a patient such that survival of oligodendrocytes is increased.
US20060189544 Integrin-Mediated drug targeting The present invention relates to cytostatics which have a tumour-specific action as a result of linkage to αvβ3 integrin antagonists via preferred linking units. The preferred linking units guarantee serum stability of the conjugate of cytostatic and αvβ3 integrin antagonist and at the same time the desired intracellular action in tumour cells as a result of their enzymatic or hydrolytic cleavability with release of the cytostatic.
CA2856759A1 3-phenyl-isoquinolin-1(2h)-one derivatives as parp-1 inhibitors There are provided substituted 3-phenyl-isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly(ADP-ribose) polymerase PARP-1 with respect to poly(ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
WO2011011632A1 Methods and compositions for modulating membrane potential to influence cell behavior The present invention provides methods for controlling proliferation, differentiation, and/or migration of cells by modulating membrane potential through an endogenously expressed channel protein. The present invention also provides methods for identifying candidate instructor cells, as well as therapeutic agents that are useful for modulating (e.g., promote or inhibit) proliferation and differentiation, as well as promoting regeneration of a desired tissue type.
US20100222410 Nuclease compositions and methods The present invention generally relates to various nucleases and uses thereof, and in some cases, to the UPF0054 protein superfamily. Members of the UPF0054 protein superfamily, such as the E. coli protein YbeY, may possess RNase activity and may be involved in certain important cellular processes. Disruption of YbeY activity can lead to increased sensitivity to antibiotics. Accordingly, certain embodiments of the invention are directed to systems and methods for screening target compounds for activity against UPF0054 superfamily proteins. In some embodiments, the screening method allows to target compositions to be determined that show selective activity against UPF0054 superfamily proteins. Other embodiments of the invention provide for nucleases capable of site-specific cleavage of nucleic acids.
WO2014071426A1 Alum for treating skin diseases Preparation containing alum, in particular ammonium alum, for treating skin diseases, in particular eczemas such as atopic dermatitis and psoriasis, said preparation containing alum, in particular ammonium alum, dissolved in double-distilled water.
US7265107 For therapy and prophylaxis of microbial infections The current invention relates to a series of rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms, specifically, the 3,4-cyclo-rifamycin derivatives having an oxime group at the C-11 position.
WO2014123894A1 Macrocyclic compounds as hcv entry inhibitors Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
CN103340879A Medical application of 11-ketoandrostenedione and 11-ketotestosterone The invention relates to medical application of 11-ketoandrostenedione and 11-ketotestosterone, in particular relates to application of a type I 11beta-hydroxysteroid dehydrogenase (11beta-hydroxysteroid dehydrogenase type I, HSD11B1) dual regulator, wherein dual regulation means that HSD11B1 reductase is inhibited while HSD11B1 oxidase is activated. The 11-ketoandrostenedione and the 11-ketotestosterone disclosed by the invention can be used for preparing androgen replacement treatment medicines, glucocorticoid hormonosis treatment medicines and hypogonadotropic hypogonadism dysfunction and/or sterility treatment medicines.
WO2006133634A1 Tetrahydroindole derivatives and tetrahydroindazole derivatives, and use thereof Compounds of formula (I) and salts thereof are provided, and the said compounds and salts are characterized in their activities of inhibiting the growth of tumor cells and malignant cells, such as breast carcinoma, pulmonary carcinoma, cervical carcinoma, rectal carcinoma, prostatic carcinoma, hepatic carcinoma and leucocythaemia and the like cancer cells.
US20080045504 Benzonitrile Derivatives to Treat Musculoskeletal Frailty This invention relates to novel amino substituted benzonitrile derivatives and to pharmaceutical compositions containing the novel amino substituted benzonitrile derivatives. This invention also relates to methods of treatment using amino substituted benzonitrile derivatives to prevent and/or restore age-related decline in muscle mass and strength, treat a wasting disease, treat a condition that prevents with low bone mass, increase muscle mass, increase lean body mass, decrease fat body mass, and treat bone fracture and muscle damage in mammals, including humans.
CN101264198A Jinguhuo spraying agent and preparation thereof The invention relates to a health-care product, in particular to a muscle and joint-innerve spraying agent. The invention also relates to a preparation method. Pre 1000 ml muscle and joint-innerve spraying agent is made by the active pharmaceutical ingredient and accessories in the following weight ratio, wherein, the active pharmaceutical ingredient is that: clematis root 50 to 60 g, safflower 5 to 13 g, leech 20 to 35 g, dragon's blood 40 to 50 g, olibanum 10 to 20 g, myrrh 10 to 20 g, monkshood root 15 to 25 g, barrenwort 40 to 60 g, borneol 5 to 12 g, propolis 20 to 30 g, laurocapram 8 to 12g and ethyl fiber 2 to 4 g. the invention is suitable for people with pain caused by cervical spondylosis, scapulahumeral periarthritis, protrusion of lumbar intervertebral discs, osteoarthritis, gout and herpes zoster, and people suffering from lumbocrural pain, muscle soreness and neurogenic headache. The health-care product has the advantages of releasing pain and improving microcirculation.
CN1799547A Pirenzepine eyes gel containing hyaluronic acid The invention belong to medicine preparation field, relating to a externally used eye drops containing stabilizing agent for piperilunxiping. The product contains the stabilizing agent for active component piperilunxiping, employing hyaluronic acid to increase the viscosity of the medicine, and to combine with main component and other addictive to form the eye drops, the chemical and physical property is kept stable in preparing and storing process, and the insoluble degradable substance is inhibited for generation.
US20130004588 Divalent cation containing compositions and methods for treating and/or preventing enzymatic irritation Compositions and methods for treating and/or preventing conditions such as diaper rash and atopic dermatitis are disclosed. The compositions and methods are particularly useful in the treatment and prevention of diaper rash and diaper dermatitis caused by the prolonged contact of human skin with body waste. The methods employ the topical application of a trypsin-inhibiting agent to the area in need of such treatment, or the area where prevention is desired. The trypsin-inhibiting agent is preferably a divalent cation.
EP0752005B1 Compacted nucleic acids and their delivery to cells Nucleic acids are compacted, substantially without aggregation, to facilitate their uptake by target cells of an organism to which the compacted material is administered. The nucleic acids may achieve a clinical effet as a result of gene expression, hybridization to endogenous nucleic acids whose expression is undesired, or site-specific integration so that a target gene is replaced, modified or deleted. The targeting may be enhanced by means of a target cell-binding moiety. The nucleic acid is preferably compacted to a condensed state.
CN102526038A Temozolomide brain-targeting pharmaceutical composition and application thereof The invention discloses a temozolomide brain-targeting pharmaceutical composition and application thereof. The pharmaceutical composition provided by the invention contains a therapeutic effective dose of temozolomide, an absorbefacient and a pharmaceutical carrier. The invention also provides a pharmaceutical composition which contains a therapeutic effective dose of temozolomide, a stabilizer and a pharmaceutical carrier. The invention further provides the application of the pharmaceutical compositions provided by the invention in the preparation of drugs for intranasal administration. The compositions provided by the invention can be used as nasal powder. The temozolomide nasal powder provided by the invention is formed by the temozolomide, the pharmaceutical carrier and the stabilizeror the absorbefacient and is a preparation which reaches the brain to treat brain tumors through the absorption of nasal mucosa.
CN103181890A Amikacin sulphate injection and preparation method for same The invention discloses an amikacin sulphate injection and a preparation method for the same. According to the preparation method disclosed by the invention, an antioxidant, a complexant and injection water are added in amikacin sulphate. The amikacin sulphate injection and the preparation method for the same disclosed by the invention are simple in production process and low in cost, solve the problem that the amikacin sulphate injection cannot meet the requirement of terminal sterilisation and make up the shortages of the prior art, and are suitable for modern production.
WO2005058895A1 Novel crystalline forms of 2, 3 dimethyl-8- (2, 6-dimethylbenzylamino) -n-hydroxyethyl-imidazo [1, 2-a] pyridine-6-carboxamide mesylate salt. The present invention relates to novel crystalline forms of 2,3-dimethyl-8-(2,6-dimethylbenzylamino)-N-hydroxyethyl-imidazo[1,2-a]pyridine-6-carboxamide mesylate salt and to mixture thereof. Further, the present invention also relates to processes for obtaining them, the use of said compounds for the treatment of gastrointestinal disorders, and pharmaceutical compositions containing them.
CN101084919A Potassium iodide sustained-release preparation and preparation method thereof The invention provides potassium iodide sustained release medication and its preparation method. The preparation comprises (By weight percentage) potassium iodide 10-70%, adjuvant with sustained release effect 10-90%, and other adjuvant in balance. Adjuvant with sustained release effect is glyceryl monostearate and/or beeswax and/or carnauba wax and/or stearyl alcohol and/or stearyl alcohol and/or polyacrylic resin. The preparation method comprises granulating through fusion method, coating, tabletting or capsulating to give skeleton type agents; pressing tablet core directly or taking the skeleton type tablet as core, and coating to give membrane controlled release agent. The inventive preparation has the advantages of good sustained release and controlled release and broad basic remedy content scope. Compared with common potassium iodide preparation, the preparation has the advantages of improved stability and therapeutic effect, reduced adverse reaction and administration times. Small dose of the preparation can be used for iodine supplement, and significant dose can be used for treating acute and chronic lead poisoning.
CN102038953A Composite for local anesthesia before ophthalmologic operation and preparation method and application thereof The invention discloses a composite for local anesthesia before an ophthalmologic operation and a preparation method and application thereof. Relative to the total volume of the composite, the composite comprises 0.05-0.3w/v% of sodium hyaluronate and 1.0-4.0w/v% of local anesthetic.
CN103300373A Lutein and procyanidine composite soft capsule and preparation method thereof The invention discloses a lutein and procyanidine composite soft capsule which comprises a capsule skin and inclusion therein, wherein the inclusion comprises a lutein extract, a procyanidine extract, beta-carotene, zeaxanthine, beeswax, multiple vitamins and plant oil, wherein the lutein extract is extracted from calendula; the lutein has the purity of 20 percent; the procyanidine extract is extracted from grape seeds; and the procyanidine has the purity of 95 percent. The invention also discloses a method for preparing the lutein and procyanidine composite soft capsule. The provided lutein and procyanidine composite soft capsule can be rapidly absorbed by a human body, provides enough lutein and procyanidine for the human body, can eliminate multiple free radicals, enhance the human immunity, delay senility of the body and improve the body asthenopia and can supplement calcium and zinc aiming at the Chinese constitution features, and the preparation method is simple.
CN1868482A Aspirin slow-release tablet and its prepn. method A slow-release aspirin tablet for treating transient cerebral ischemia attack, myocardial infarction, thrombosis, unstable angina pectoris, etc is proportionally prepared from aspirin, starch, hydroxypropyl methylcellulose, polyacrylic resin No.2, white dextrin, tartaric acid, tween-80 and alcohol. Its preparing process is also disclosed.
EP1723151A2 Pyrrolobenzodiazepines as key intermediates in the synthesis of dimeric cytotoxic pyrrolobenzodiazepines Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R2 and R3 are independently selected from -H, =O, =CH2, -CN, -R, OR, halo, =CH-R, O-SO2-R, CO2R and COR; R10 is a carbamate-based nitrogen protecting group; and R11 is an oxygen protecting group.
EP2069308A2 Azonafide derived tumor and cancer targeting compounds An azonafide-based compound of Formula I, a composition comprising the compound, and a method of using the compound to deliver a cytotoxic azonafide derivative to a cell, as well as related compounds and methods for the use thereof to prepare an azonafide-based compound of Formula I.
CN102058545B Meropenem freeze-dried preparation for injection and preparation method thereof The invention discloses a meropenem freeze-dried preparation for injection and a preparation method thereof. 1,000 milliliters of water for injection comprises the following ingredients: 2 to 15 grams of meropenem, 20 to 100 grams of oil for injection, 0 to 20 grams of stabilizing agent, 10 to 80 grams of emulsifying agent, 10 to 30 grams of glycerol and 50 to 200 grams of freeze-dried protectiveagent. The preparation method comprises the following steps of: dispersing the emulsifying agent into the oil for injection and adding the meropenem; adding the glycerol into the water for injection;stirring and mixing uniformly to form an aqueous phase; emulsifying and homogenizing an oil phase and the aqueous phase to obtain emulsion; and preparing freeze-dried emulsion. A meropenem lipid microsphere preparation provided by the invention can obviously reduce hydrolysis and oxidation of active ingredients and can maintain the integrity of the lipid microsphere structure so as to obviously improve the stability of medicament storage.
WO2009081208A1 Processes to pregabalin The present invention relates to a novel method for the preparation of racemic pregabalin (1) or a single enantiomer thereof, (S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid (2).
CN102614207A 18-membered ring macrocyclic compound and analogues thereof The present invention relates to an 18-membered ring macrocyclic compound and analogues thereof, broadly relates to an 18-membered ring macrocyclic antimicrobial agent named as Tiacumicins, and especially to OPT-80 (wherein the OPT-80 almost entirely comprises R-Tiacumicin B). The present invention further relates a drug composition containing the OPT-80, and a method for application of the OPT-80. Specifically, the compound is an effective drug for treatments of bacterial infections, and especially C.difficile infection.
US20120301527 Hair follicle targeting compositions This invention provides topical pharmaceutical or cosmetic compositions, and uses thereof in treating a disease or condition of the hair follicle. The compositions of this invention are emulsions of an oil-in-polyol with a mean particle size of below one micron, and further comprising at least one oil, one polyol, and one stabilizer.
US20110166190 Methods of treating mammals with eustachian tube dysfunctions The invention relates to methods of medically treating mammals with Eustachian tube dysfunctions, such as Ménière's disease, vertigo, Otitis Media (including Otitis Media with Effusion (OME), Acute Otitis Media (AOM) and Aerotitis Media (AM)) as well as other disorders which are characterized by ET dysfunction.
US20090012169 Combined use of L-carnitine, acetyle L-carnitine and propionyl L-carnitine for the treatment of oligoasthenoteratospermia L-carnitine, acetyl L-carnitine and propionyl L-carnitine inner salts, or their pharmaceutically acceptable salts, are used in combination to treat oligoasthenoteratosperia including oligospermia, asthenospermia, and teratospermia.
CN101518521A New medical application of cedrol The invention relates to new medical application of cedrol (CE), in particular to new application thereof in preparing medicaments for relieving pain and treating arthritis. The cedrol is alpha-cedrol, beta-CE or raceme of the two in any proportion, and the total effective dose of the cedrol is between 1 and 100 mg/kg/d. The CE is extracted from natural plants extensive in sources. The invention adopts rat-paw chondrus inflammation-inducing method and adjuvant arthritis to observe the anti-inflammatory effects of the CE, and results show that the CE has obvious effect of inhibiting nonspecific inflammation reaction caused by carrageenin and also has remarkable effect of treating and preventing the adjuvant arthritis. The invention adopts a tail-flick method to observe the analgesic effects of the CE, and results show that the CE has remarkable analgesic effects on the light-heat stimulated tails of rats. The invention provides a raw material for anti-inflammatory and analgesic drugs, which is exact in therapeutic effects, safe, convenient and extensive in sources, and can be combined with one or more pharmaceutically acceptable carriers so as to prepare a cedrol pharmaceutical composition or preparation.
EP1847535A1 1-(piperidin-4-yl)-1h-indole derivative The present invention provides a compound represented by the formula (1) or a pharmacologically acceptable salt thereof, or a hydrate thereof (provided that a compound in which all of R4a, R4b, and R4c are hydrogen atoms is excluded.): [wherein R1 represents a hydrogen atom, R2 represents a hydrogen atom, R3 represents the formula: wherein R4a, R4b, and R4c are the same as or different from each other and each represents a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group, etc.]
CN1835937B Novel thiazoline derivatives as selective androgen receptor modulators (SARMS) The present invention is directed to novel thiazoline derivatives of the general formula (I); wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
EP1935420A1 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors The present invention relates to 2-adamantyl-butyramide derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11 β-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
US8741259 Low molecular weight thyroid stimulating hormone receptor (TSHR) agonists Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
US20130089587 Personal Care Compositions and Methods of Making Same The present invention relates to a personal care composition and methods of using the same, the composition including an anionic surfactant, a cationic conditioning polymer, and a silicone emulsion wherein a total content of a cyclic polysiloxane having a general formula: is present in the silicone emulsion in an amount less than 2.5 wt % based on the total weight of all polysiloxanes, R is a substituted or unsubstituted C1 to C10 alkyl or aryl, wherein m is 4 or 5, wherein the composition forms coacervate particles upon dilution with water, and wherein a percentage of the coacervate particles with a floc size of greater than about 20 micron is from about 1% to about 60% upon dilution with water.
US20090326055 Chroman-Derived Compounds For The Treatment Of Cancer The present invention provides methods for inhibiting the growth of androgen-independent prostate cancer tumor cells in a human comprising administering to the human. The invention further provides pharmaceutical and nutraceutical compositions containing chroman-derived compounds useful in the alleviation of cancer.
WO2007039616A1 Pharmaceutically active tetrahydro-pyrrolo[1,2-b]isothiazole 1,1-dioxides 3a,4,5,6-Tetrahydro-pyrrolo1 ,2-b]-isothiazoles wherein the sulphur is in the form of a dioxide and their use for the treatment or prevention of disorders mediated by interactions of LFA-1 with its ligands involved in cell adhesion, migration and activation.
US20120164145 H. pylori lipopolysaccharide outer core epitope Helicobacter pylori, one of the most common human pathogens, is associated with the development of human chronic gastritis, peptic ulcers and gastric cancer. The invention relates to a α1,6-glucan-containing Helicobacter pylori compound comprising the structure of Formula (I): wherein R is a α-DDHep-3-α-L-Fuc-3-β-GlcNAc trisaccharide substituted with an α1,6-glucan linked to an α1,3-DD-heptan, and wherein the last DD-Hep residue of α1,3-DD-heptan is capped with β-GlcNAc residue. Compositions comprising the compound, uses of the compound, and antibodies raised against the compound are also described.
CN101185634A Topotecan sustained-release implant for treating solid tumor A topotecan sustained release implant includes effective dose of anticancer topotecan, sustained release excipients and a certain quantity of sustained release moderator. Solid tumors include pancreatic cancer, lung cancer, liver cancer, breast cancer, cerebroma, ovarian cancer, prostatic carcinoma, esophageal carcinoma, lymphadenoma, osteosarcoma and colorectal cancer. Sustained release excipients are mainly one or combination of poly(L-lactide-co-ethyl phosphate), poly (L-lactide-co-phosphoric acid propyl), the copolymer of glycolic acid and hydroxyacetic acid and polifeprosan; in the process of decompression, topotecan can be slowly released to local tumor, thus maintaining effective drug concentration of local tumor as well as significantly reducing overall toxic reaction. Being placed in local tumor, the sustained release implant not only reduces overall toxic reaction of tepotecan, but also selectively improves drug concentration in local tumor, enhancing the therapeutic effects of non-operative therapy such as chemotherapy drugs and radiotherapy.
CN103622939A Application of compound for preparing drugs treating osteoarthritis The invention discloses new application of Trichostatin A treating the osteoarthritis. The osteoarthritis is one of the serious diseases harmful to human health; with the aging of the population, the number of patients suffering from the osteoarthritis is increased day by day, which brings the world an enormous social, medical and economic burden; although the relevant experts and scholars attach great importance to the prevention and the treatment of the disease, effective therapeutic drugs are still unavailable. Tests in vitro show that Trichostatin A has a significant anti-osteoarthritis effect. Experimental results show that Trichostatin A can suppress the expression of protein MMP3, protein MMP13 and mRNA induced by IL-1 in a human chondrosarcoma cell SW1353, and the suppressing effects are dose-dependent, so that the compound has a therapeutic effect on the osteoarthritis.
CA2835798A1 Epha4 is a disease modifier in motor neuron disease The present application relates to the field of motor neuron diseases, most particularly to amyotrophic lateral sclerosis and spinomuscular atrophy. Provided herein are strategies to improve symptoms and increase survival in patients with these axonopathies by inhibiting signaling mediated by the EphA4 ephrin receptor.
US20100151032 Silver and Zinc Containing Body Care Agent The invention relates to a body care agent containing metal particles which release zinc and silver ions in said body care agent by contacting body liquid or body humidity and whose metallic silver content at least equal or greater than 99 % (m/m).
US20090048194 Vagal Afferent Neurons as Targets for Treatment A method of identifying a compound capable of reducing or preventing prolonged sensory neuron hyper-excitability comprising the steps of: (a) administering the compound to an experimental non-human animal having prolonged sensory neuron hyper-excitability; (b) generating an expression profile of the genes modulated in the Nodose Ganglia (NG) of the animal of step (a); (c) comparing the expression profile obtained in (b) with the expression profile of a corresponding panel of genes expressed in the NG of an experimental non-human animal having no prolonged sensory neuron hyper-excitability; wherein a positive correlation of the expression profiles is indicative that the compound is capable of reducing or preventing prolonged sensory neuron hyper-excitability in NG.
US20080045454 Polynucleotide encoding a TRIM-cyp polypeptide, compositions thereof, and methods of using same The invention provides an isolated nucleic acid encoding a TRIM—cyclophilin A fusion sequence encoding a TRIMcyp fusion protein which is active as an anti-viral agent, and in particular an anti-HIV-1 agent. The invention provides for a nucleic acid encoding a polypeptide having both TRIM activity and cyclophilin activity. The invention provides for an isolated polynucleotide encoding a TRIM-cyclophilin fusion protein, or variants thereof retaining the TRIM and cyclophilin activities. The invention provides for compositions thereof, antibodies that specifically bind thereto, and vectors and host cells comprising the nucleic acid or polypeptide. In addition, the invention provides for methods for treating or preventing viral infection, or reducing viral load in a subject comprising administering the nucleic acid, polypeptide, vector, or composition to the subject in an amount effective to treat or prevent the viral infection. In some embodiments, the viral infection is HIV-1 infection, hepatitis C infection, pox virus infection, vaccinia virus infection, or HTLV infection.
US20090326000 Resveratrol formulations and methods of use A method is provided for preventing or treating obesity and for reducing the percentage body fat content of an individual. The method involves administration, preferably topical administration, of an active agent selected from the group consisting of resveratrol, pharmacologically acceptable salts, esters, amides, and analogs thereof, and combinations of any of the foregoing. Topical formulations for use in conjunction with the method for reducing the percentage body fat content of an individual are provided as well.
US20120309757 N-biphenylmethylindole modulators of pparg The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
US20110160191 New fused polycyclic compounds having a heterocyclic ring(s) and pharmaceutical use thereof The present invention provides a fused polycyclic compound of the following formula, analogues thereof and pharmaceutically acceptable salts thereof; and agents for increasing the sugar-transporting capacity, hypoglycemic agents and pharmaceutical compositions containing the above compounds. This fused polycyclic compound has high medicinal properties and few side-effects, and a therapeutic effect on diabetes. wherein R represents an alkoxy group, R′ represents an oxazolylpropionyl group or a thiazolylpropionyl group, and R″ represent a hydrogen atom.
US20100120716 Macrocyclic hepatitis c serine protease inhibitors and uses therefor Macrocyclic inhibitors of Hepatitis C protease are provided, the inhibitors including a boronic acid or ester group, a macrocyclic ring of about 13 to 25 atoms including at least two amide linkages, a proline-analogous group, and a connecting segment joining moieties on either side of the proline-analogous group. Methods of making the HCV protease-inhibitory compounds, methods of using the compounds, formulations of the compounds, and pharmaceutical combinations including the compounds, are provided.
EP0850068B1 Lipid extract having anti-inflammatory activity Anti-inflammatory, and particularly anti-arthritic, treatment of a human or animal patient comprises administration to the patient of an effective amount of a lipid extract of Perna canaliculus or Mytilus edulis.
CN102755286A Gentamycin sulfate injection containing buffer agent The invention discloses gentamycin sulfate injection containing a buffer agent. Each milliliter of injection consists of 18 to 45 milligrams of gentamycin sulfate, an antioxidant, a pH buffer agent and the balance of injection water, wherein the antioxidant is one of sodium sulfite, sodium bisulfite or sodium pyrosulfite. The injection is characterized in that the pH value of the pH buffer agent is 5.5 to 6.0.
WO2013017548A1 1,4-diaryl-2-azetidinones with anti-tumoral activity Disclosed are compounds of formula (I): wherein one of A and B is the group:(II) wherein R1 is selected from H and OCH3, and the other is the group:(III) wherein R2 is selected from H, OH, NO2, NH2; R3 is selected from OH and NH2;15 the salts, enantiomers and diastereoisomers thereof; with the exclusion of the following compounds: 3,4-cis-3-hydroxy-4-(3-nitro-4-methoxyphenyl)-1-(3,4,5- trimethoxyphenyl)azetidin-2-one; 3,4-cis-4-(3-amino-4-methoxyphenyl)-3-hydroxy-1-(3,4,5-20 trimethoxyphenyl)-azetidin-2-one; for use as antitumor agents.
WO2014034902A1 Amine salt and crystals thereof Provided is a compound that can serve as a drug for the treatment of underactive bladder, which can be administered orally and poses little risk of side effects. Also provided are crystals that are advantageous as the bulk drug of a pharmaceutical in terms of stability, long-term storage, ease of handling, ease of formulation, and the like. Salts of 2-[(2-{(1R,5R)-2-oxo-5-[(1E,4S)-7,8,8-trifluoro-4-hydroxy-4-methyl-1,7‑ octadien-1-yl]cyclopentyl}ethyl)thio]-1,3-thiazole-4-carboxylic acid, or a mixture of diastereomers thereof, and 4-piperidinemethanol are extremely chemically stable crystals and therefore permit long-term storage and are very useful as the bulk drug of a pharmaceutical.
WO2013187395A1 Tablet having ingestion easiness and dividability A tablet which is easy to ingest, contains 500 mg of levofloxacin, has a mass of 570 to 700 mg, a projected area of 90 to 125 mm2 on a plan view and a hardness of 30 to 300 N, and can be divided easily.
CN101069532A Blended oil in which the ratio of linoleic acid and linolenic acid is 4:1 The present invention provides a Quanjiafu health-care blend oil containing linoleic acid and linolenic acid. Said blend oil is formed from five vegetable oils of perilla oil, flax-seed oil, corn oil, rapeseed oil and soybean oil. In said blend oil the necessary fatty acid content is 40% of its total weight, in which the linoleic acid content is 32% and the linolenic acid content is 8%.
US7189518 Soluble CD40L(CD154) as a prognostic marker of atherosclerotic diseases This invention involves the new use of a diagnostic test to determine the risk of atherosclerotic diseases such as myocardial infarction and stroke, particularly among individuals with no signs or symptoms of current disease and among nonsmokers. Further, this invention involves the new use of a diagnostic test to assist physicians in determining which individuals at risk will preferentially benefit from certain treatments designed either to prevent first or recurrent myocardial infarctions and strokes, or to treat acute and chronic cardiovascular disorders. Methods for treatment also are described.
EP1082112B1 Endogenous nitric oxide synthesis under conditions of low oxygen tension The present invention provides methods of promoting synthesis of nitric oxide or endothelium-derived relaxing factor (EDRF) in hypoxic mammalian tissues by administering at least one N-hydroxyguanidine compound that is a substrate of nitric oxide synthase, and, optionally, one or more vasoactive agents. The present invention also provides methods of promoting relaxation of vascular and non-vascular smooth muscle and treating sexual dysfunctions in patients by administering at least one N-hydroxyguanidine compound that is a substrate for nitric oxide synthase, and, optionally, one or more vasoactive agents. The present invention also provides methods for treating clinical conditions resulting from hypoxic conditions, such as pulmonary disease, cardiovascular disorders, circulatory hypoxia, specific organ hypoxia, localized hypoxia, edema, central nervous system disorders, memory loss, or arterial disease. The present invention also provides methods for treating clinical conditions associated with deficient nitric oxide pathways by administering at least one N-hydroxyguanidine compound and, optionally, one or more vasoactive agents. The present invention also provides pharmaceutical compositions comprising at least one N-hydroxyguanidine compound and, optionally, one or more vasoactive agents.
CN102827206A Pradefovir crystal The invention discloses a crystal of (+)-cis-9-(2-(4-((S)-(3-chlorphenyl)-2-oxygen-1, 3, 2-dioxo phosphorus heterocyclic hexa-ring-2-methylene)-1-ethyl) adenine mesylate (Pradefovir), a drug of the crystal, a preparation method of the crystal and the like.
US20080214513 Reducing granulation tissue in humans having otitis and an open tympanic membrane (otitis media) by topically applying an aqueous suspension composition of ciprofloxacin and dexamethasone Aqueous suspension formulations containing dexamethasone and ciprofloxacin are disclosed for the treatment of middle ear infections in human patients having an open tympanic membrane.
EP2685970A1 Composition comprising a diindolylmethane and a retinoid to treat a skin condition Provided is a composition for use in treating a skin condition, the composition comprising: (a) a first component comprising a substituted or unsubstituted diindolylmethane compound; and (b) a second component comprising a substituted or unsubstituted retinoid compound.
US20060251651 Antagonist and agonist which bind to a strong binding site of chemokine receptor An antagonist or an agonist which binds to a strong binding site of CCR5; a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer which comprises the same; a method for screening a compound which binds to a strong binding site of CCR5; a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer which comprises the antagonist or the agonist selected by the screening method; an antagonist or an agonist which binds to a strong binding site of a chemokine receptor; a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer which comprises the same; a method for screening a compound which binds to a strong binding site of a chemokine receptor; and a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer which comprises the antagonist or the agonist selected by the screening method. The antagonist or the agonist of the present invention is useful as a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer.
CN1788725A Voriconazole freeze-drying powder injection and its preparation process The present invention relates to one kind of freeze dried voriconazole composition including voriconazole in effectively treating amount and hydroxypropyl-beta-cyclodextrin. Each of the preparation unit contains voriconazole in 50-400 mg, pregreably 200 mg and hydroxypropyl-beta-cyclodextrin of 5-40 time, preferably 15-25 times, weight of voriconazole.
US7316900 Comprises methylated antisense oligonucleotide sequence for regulation of urokinase type plasminogen activator and treatment of cancer The present invention provides a method of regulating the expression of the urokinase type plasminogen activator (“uPA”) gene in a mammalian cell comprising the steps of: identifying a target nucleotide sequence in a gene of interest, obtaining a methylated antisense oligonucleotide sequence complementary to the target sequence, said oligonucleotide sequence having 5 methylated cytosine in place of unmethylated cytosine in the region complementary to the CpG region in the target nucleotide sequence, and exposing the cell to copies of the oligonucleotide sequence under suitable conditions, such that the oligonucleotide sequence enters the nucleus and interacts with the target sequence to promote methylation of the target nucleotide sequence.
EP2691396A2 Enopeptins, uses thereof, and methods of synthesis thereto Provided herein are inventive enopeptin compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Further provided are methods of preparation, use, and treatment.
EP2385054A1 Cefdinir acid double salt and its preparation The invention provides an acid double salt of cefdinir. The acid double salt is obtained by reacting cefdinir with acid and alkali metal element or ammonium (including ammonia) compound or with acid salt. The cefdinir sulfate double salt is prepared when acid or acid salt is sulfate. The cefdinir phosphate double salt is prepared when acid or acid salt is phosphate. The cefdinir acid double salt of the present invention has the obvious advantages of good solubility and high bioavailability, and can be prepared into oral solid preparation or injection. The cefdinir acid double salt has the following structural general formula.
CN101579460A Weight loss pill for external application The invention discloses a weight loss pill for external application in the field of medicaments, which consists of 10 to 30g of rhizoma cyperi, 10 to 30g of alisma orientale, 10 to 30g of Chinese angelica, 10 to 30g of betelnut, 10 to 30g of borneol, 10 to 30g of fennel, 10 to 30g of oriental waterplantain leaf, and 10 to 30g of rhizoma atractylodis. The weight loss pill for external application is applied to abdomens of human bodies to make medicinal components permeate into the skin of the human bodies under the action of message and hot compression to achieve the effects of improving the metabolism, promoting the microcirculation as well as the absorption and transformation of fat. The weight loss pill for external application has the characteristics of convenient use, obvious effect, no rebounce and no need of food control. The weight loss pill for external application is suitable for obese patients to lose subcutaneous fat and reduce body weight.
CN102898379A N-(4-(4-(3-chlorphenyl)piperazino-1-yl)pyrimidyl-2-yl)amide or its salts, and preparation method and use thereof The invention discloses N-(4-(4-(3-chlorphenyl)piperazino-1-yl)pyrimidyl-2-yl)amide. The N-(4-(4-(3-chlorphenyl)piperazino-1-yl)pyrimidyl-2-yl)amide has a structural formula (I). In the structural formula (I), R represents a group shown in the patent specification; when X2 represents -CH3, X1 represents any one of -H, -Br and groups shown in the patent specification; when X2 represents -H, X1 represents any one of -H, -Br and -Cl; X3 represents any one of -H and a group shown in the patent specification; and X4 represents -H. The invention provides pharmaceutically acceptable organic salts or inorganic salts of N-(4-(4-(3-chlorphenyl)piperazino-1-yl)pyrimidyl-2-yl)amide, wherein the pharmaceutically acceptable organic salts comprise a methanesulfonate, a sulfonate, a formate, an acetate, a malate and a lactate and the pharmaceutically acceptable inorganic salts comprise a hydrochloride, a sulfate and a phosphate. The invention also discloses a preparation method of N-(4-(4-(3-chlorphenyl)piperazino-1-yl)pyrimidyl-2-yl)amide and a use of N-(4-(4-(3-chlorphenyl)piperazino-1-yl)pyrimidyl-2-yl)amide and its pharmaceutically acceptable salts in preparation of antitumor drugs and especially in preparation of drugs for treating lung, liver, stomach and nasopharynx cancers.
EP1131312B1 Novel pyrimidine derivatives and processes for the preparation thereof The present invention relates to novel pyrimidine derivatives and pharmaceutically acceptable non-toxic salts thereof which possess an excellent inhibitory activity against gastric acid secretion, a pharmaceutical composition containing the same as an active ingredient, and a process for the preparation thereof.
US20110318394 Multi-linked star-shaped polymers and synthetic methods therfor The invention describes new synthetic medical adhesives and antifouling coatings which exploit the key components of natural marine mussel adhesive proteins.
EP2716290A1 Dry-coated tablet containing tegafur, gimeracil and oteracil potassium The present invention provides a dry-coated tablet comprising: an inner core containing, as active ingredients, (a) tegafur, (b) gimeracil, and (c) oteracil potassium; and an outer shell.
WO2010122578A3 Process for preparation of sitagliptin and its intermediates Improved processes for the preparation of Sitagliptin compound of formula-1 and its intermediates are provided.
US20070179139 Methyl 4-{[(2-{4-[(4-bromophenoxy)methyl]-2,5-dimethyl-3-thienyl}ethyl)(5-ethoxy-5-oxopentyl)amino]methyl}benzoate, for example; treatment of cardiovascular and other diseases The invention relates to compounds of formula (I) and their salts and stereoisomers in which the variables are as defined in the description and claims, for producing medicaments used in the treatment of cardiovascular and other diseases. Such compounds, processes for preparing them, compositions containing them, and methods of using them are claimed.
CN102727500A Compound aminophylline rapidly disintegrating oral tablet The invention discloses a compound aminophylline rapidly disintegrating oral tablet and its preparation technology and belongs to the field of veterinary drug preparation. The compound aminophylline rapidly disintegrating oral tablet provided by the invention is prepared from the following components of: by weight, 25-200 parts of aminophylline, 1-8 parts of Vetmedin, 150-400 parts of a disintegrating agent, 270-750 parts of a diluent, 70-100 parts of polyvinylpyrrolidone K30, 2-10 parts of a lubricant, 2-12 parts of menthol and 100 parts of camphor. In comparison with other inventions, the compound aminophylline rapidly disintegrating oral tablet provided by the invention can more comprehensively treat cardiogenic cough and asthma of old dogs and cats. The rapidly disintegrating oral tablet prepared by direct compression can be convenient for drug administration, thus bringing great convenience for the application in pet clinic.
EP1210348B9 Naphthyridine derivatives, processes for their preparation, their use and pharmaceutical compositions comprising them The present invention relates to compounds of formula (I), in which B, G, Z, X, Y, r, s and t have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
US7476380 Using vitamin A and/or the derivatives and/or the esters for therapy and prophylaxis, side effect reduction The invention describes a means for the treatment of diseases of the tracheo-bronchial tract, particularly of COPD.
CA2214431C Human vegf-specific antisense oligonucleotides Disclosed are oligonucleotides complementary to VEGF-specific nucleic acid useful in reducing the expression of VEGF. Also disclosed are pharmaceutical formulations containing such oligonucleotides and method useful for treating various disorders associated with neovascularization and angiogenesis.
CN102659742A Application of genistein derivative in preparing medicament for treating learning and memory disorder The invention belongs to the field of chemical pharmaceutical technology, and in particular relates to application of a genistein derivative 4', 5'-dyhydroxy-7-[4-(N, N-diethylamino) butoxy] isoflavone in preparing a medicament for treating learning and memory disorder. 4', 5'-dyhydroxy-7-[4-(N, N-diethylamino) butoxy] isoflavone has the effect of promoting macrophage chemotactic fator (MCF)-7 cell proliferation and the action effect is in a bell jar type. The latent time of female castrated mice (oophorectomy is performed) in a water maze experiment is shortened and the error time of the mice is greatly decreased in a Y maze experiment. The fact indicates that 4', 5'-dyhydroxy-7-[4-(N, N-diethylamino) butoxy] isoflavone can effectively improve learning and memory capability. The improvement of learning and memory is consistent with the enhancement of phosphorylation of calcium-calmodulin dependent protein kinase (CaMk) II. 4', 5'-dyhydroxy-7-[4-(N, N-diethylamino) butoxy] isoflavone has good effects of improving learning and memory and can be used for preparing the medicament for improving learning and memory.
US20100210604 Zwitterion solution for low-volume therapeutic delivery A formulation is provided that includes a volume of an aqueous multivalent physiological ion solution compatible with cerebrospinal fluid containing at least one divalent cation of magnesium or calcium, and at least one anion of carbonate or phosphate, and having a pH between 6.5 and 8.0. A zwitterionic therapeutic agent other than baclofen is dissolved the solution to achieve higher concentration or ease of solution and/or storage relative to therapeutic saline solutions of the same agent. A process of delivering a zwitterionic therapeutic agent into a subject is provided that includes dissolving a therapeutic amount of the zwitterionic therapeutic agent in a volume of artificial cerebrospinal fluid to form a stable formulation. The solution is then administered to the subject using an intrathecal pump.
CN102872019A Efavirenz preparation adopting micronization technology The invention discloses an efavirenz preparation adopting a micronization technology. The invention provides a modified efavirenz orally-taken preparation which is used for inhibiting human immunodeficiency virus (HIV), preventing or treating HIV infection, and treating acquired immunodeficiency syndrome (AIDS) caused by the HIV infection, and in particular relates to tablets or a capsule which comprises efavirenz, wherein a micronization technology which can promote the dissolution velocity of the efavirenz in gastrointestinal tract, so that the absorption velocity and the absorption extent of the efavirenz in bodies is involved.
WO2005000838A1 4-(aminomethyl)-piperidine benzamides as 5ht4-antagonists The present invention is concerned with novel compounds of formula (I) having 5HT4-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds as well as the use as a medicine of said compounds.
WO2013016452A3 Cancer treatment using bmp inhibitor Methods for regulating cancer cell growth and survival, inhibiting cancer cell growth, promoting cancer cell death, and/or treating a cancer make use of antagonists of a type I BMP receptor. In some embodiments the cancer is a lung cancer and the cancer cell is a lung cancer cell.
CN101254298A Hoarfrost agent for antioxidation and improving human body immunity and method of preparing the same The invention discloses a cream for anti-oxidation and improvement of the human immunity and a preparation method thereof, the invention is the cream which is prepared by taking metallothionein, coenzyme-Q10 chelate lipoic acid, sclareol, chamomile, L-carnitine, rosemary oil, cimicifuga racemosa, dextran, Kamm, jojoba oil, distilled water and collagen protein as raw materials, the cream has the advantages that the effects can be improved by a plurality of times of the effects before the chelation by the organic compound formula of a plurality of anti-oxidation natural organisms for improving the human immunity, such as, MT, coenzyme-Q10 chelate and so on, thus having good improving effects on swollen welling-abscess, rhinitis and asthma which are caused by the damages of the immune system and having great eliminating effect on the prevention of the tumors; furthermore, the skin can be moisturized, whitened and replenished with water by smearing the cream of the invention.
CN103720671A Enteric preparation for proton pump inhibitor and preparation method thereof The invention relates to an enteric preparation for a proton pump inhibitor and a preparation method thereof. The preparation comprises 30mg of lansoprazole. The preparation method comprises preparation of lansoprazole enteric pellets and preparation of enteric pellet tablets, wherein each enteric pellet comprises a medical active pellet core, an isolation layer and an enteric coating. The lansoprazole enteric pellet tables prepared by the method are suitable for treating duodenal ulcer, gastric ulcer, reflux esophagitis, Zollinger-Ellison syndrome and the like. Furthermore, the pellets can be pressed into tablets, the pellets are isolated from air, and the stability of the pellets can be improved; the enteric preparation has the advantages of small size, separable dosage and the like, and the compliance of patients can be improved.
EP1940379A2 Methods for treatment of hemorrhagic shock and related disorders The present invention relates to the use of certain agents for the treatment of hemorrhagic shock and surgical procedures involving a cardiopulmonary by-pass machine. The present invention also comprises methods of preventing, treating, administering and formulating agents that prevent and/or alleviate cellular and tissue damage associated with hemorrhagic shock and surgical procedures involving a cardiopulmonary by-pass machine.
US20110178178 Treatment of Motor Fluctuations The invention relates to the use of compounds that enhance 5-hydroxytryptamine 1a receptor activity, or activation (e.g. a selective 5-hydroxytryptamine 1a receptor agonists) for preventing or reducing motor fluctuations associated with dopamine replacement therapy.
CN101700229A Prostaglandin E1 long-circulation fat microsphere preparation for intravenous injection and preparation method thereof The invention relates to a formula and a preparation method of a prostaglandin E1 long-circulation fat microsphere for intravenous injection. The preparation comprises the following components: (1) a prostaglandin E1 medicine; (2) vegetable oil (dissolving oil diluted by a medicine); (3) an emulsion surfactant; (4) an emulsion preparation stabilizing agent, an emulsifying agent, a particle diameter control agent and a polyoxyalkylene phospholipid derivative increasing the half life of the fat microsphere in blood; (5) oleic acid or oleate which is used as the emulsion preparation stabilizing agent or the emulsifying agent; (6) an antioxidant; and (7) a complex compound (glycerol) controlling the cation concentration.
CN101745120A Application of miRNA-320 in preparing preparation for promoting apoptosis of tumor cells The invention relates to the technical field of biomedicine materials, in particular to application of miRNA-320 in preparing preparation for promoting apoptosis of tumour cells, wherein the miRNA-320 is a small RNA molecule. Through experiment, the miRNA-320 restrains the growth of tumor cells and prompts the apoptosis of the tumor cells through acting on a target gene, i.e. the myelocytic leukemia gene-1(Mcl-1) and preventing the gene from expressing corresponding protein. Therefore, the miRNA-320 can be used for preparing preparations for promoting the apoptosis of the tumor cells.
EP1983978A2 Novel application of topical anesthetics for modulation of neurogenic tremor A method of ameliorating neurogenic tremor in mammals, which comprises topically administering to a mammal, which has been diagnosed with a neurogenic tremor, an effective amount of a topical anesthetic.
CA2356240C Combinations of cholesteryl ester transfer protein inhibitors and bile acid sequestering agents for cardiovascular indications The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia and atherosclerosis. Combinations disclosed include a cholesteryl ester transfer protein inhibitor combined with a bile acid sequestrant.
US20100104642 Hydrophilic foam and pharmaceutical dosage form employing the same Disclosed herein is a hydrophilic foam. The hydrophilic foam includes a polyurethane matrix having a plurality of cells. The cells are capable of retaining water in an amount of least about 8 grams of water per gram of the hydrophilic foam.
US20100249107 Biomarkers for Alzheimer's Disease Progression This invention relates generally to the analytical testing of tissue samples in vitro, and more particularly to aspects of genetic polymorphisms associated with the conversion from Mile Cognitive Impairment to dementia, e.g., Alzheimer's Disease (AD). The invention provides AD-associated mutations which are useful in the diagnosis, prognosis or therapeutic treatment of dementia, e.g., Alzheimer's Disease.
WO2010041144A2 Beta-hydroxy-gamma-aminophosphonates and methods for the preparation and use thereof The present invention provides β-hydroxy-γ-aminophosphonates, β-amino-γ- aminophosphonates, and analogs thereof that inhibit carnitine acyltransferases. The invention also provides compositions comprising these β-hydroxy-γ-aminophosphonates, β-amino-γ- aminophosphonates, and analogs, and methods of the use of such compounds and compositions in the treatment, amelioration or prevention of pathological conditions, diseases or disorders that are linked with fatty acid metabolism, such as non-insulin dependent diabetes or obesity. The invention also provides processes for the preparation of such compounds and compositions.
WO2009089442A1 Use of cranberry derivative and d-mannose composition for preventing, controlling and ameliorating urinary tract infections A use is disclosed that prevents, controls and ameliorates urinary tract infections caused by E-coli by administering a therapeutically effective amount of a human dietary supplement composition comprising a cranberry derivative or proanthocyandin containing concentrate and D-mannose combined in a form suitable for oral consumption. The cranberry derivative or proanthocyandin containing concentrate comprises from about one percent (1.0%) by weight to about 95 percent (95.0%) by weight on a dry weight basis. The composition is formulated for delivering a D-mannose unit dosage between about 0.5 to about 5.0 grams per dose and further comprising a diuretic and wherein the composition formed from the cranberry derivative or proanthocyandin containing concentrate, D-mannose and diuretic are effective together for binding to E-coli to aid in flushing the E-coli from the urinary tract system while preventing binding of E-coli to cells in the urinary tract system.
US20070269515 Probiotic Tablet Formulations A probiotic tablet comprising a probiotic micro-organism and other nutritionally active ingredients in two zones, a first zone comprising said probiotic micro-organism and prcicrably selenium, and a second zone comprising at least one said other active ingredient such as iron, other minerals and vitamin B6 kept separated from the probiotic micro-organism of said first zone, the water activity in said probiotic micro-organism containing first zone being no greater than 0.2 and the water content of said tablet being as much as 3% by weight. Good viability of the micro-organisms is obtained despite the relatively high overall moisture content.
WO2008017670A8 Pyrrolo [3, 2 -d] pyrimidines as dpp-iv inhibitors for the treatment of diabetes mellitus The present invention relates to substituted pyrrolo[3,2-d]pyrimidines of formula (I), wherein R1 and R2 are defined as in claim 1, including the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
CN103638502A Medicament for treating behcet disease and preparation method of medicament The invention discloses a medicament for treating behcet disease and a preparation method of the medicament. The medicament is mainly prepared from rhizoma curculiginis, tripterygium glycosides, honeysuckle stem, amomum tsao-ko, dark plum, gecko, dandelion, carpesium abrotanoides, talc, juncus effuses, feather cockscomb seed and the like in a certain weight ratio. The medicament has the efficacies of clearing heat, stopping blood, killing pests and diminishing inflammation, and has a quick effect and a good treatment effect when the medicament is used for treating the behcet disease; the behcet disease does not relapse after being cured.
WO2012037834A1 5α-ANDROSTANE (ALKYL)-3β,5,6β-TRIOL INJECTION AND PREPARATION METHOD THEREFOR A 5α-androstane (alkyl)-3β,5,6β-triol injection and preparation method therefor, the injection whereof using hydroxypropyl-β-cyclodextrin as a solubilizer and the active ingredient whereof being present preferably in a proportion by weight of 1-20:40-500 to the cyclodextrin. The injection may also comprise 1-100 parts of an isotonic regulator, 0-200 parts of a lyophilized filler, 0-2000 parts of a solvent. The preparation method comprises separately and successively dissolving the hydroxypropyl-β-cyclodextrin solution, the active ingredient and other soluble accessory ingredients in the water for injection, then after decolorization, depyrogenation, filtering, and sterilization of the filtrate, a liquid injection solution is obtained. Drying the filtrate yields a solid for injection.
US8580776 Compositions and methods for treating neurodegenerating diseases This invention provides agents, compositions, pharmaceutical compositions and methods for treating or slowing the progression of a neurodegenerating disease, such as Alzheimer's disease and a demyelinating disease.
CN1994279A Preparation process of irinotecan hydrochloride liposome for injection The invention relates to a method for producing injection alcaine liposome, wherein it comprises that: dissolving liposome mixture into organic solvent; mixing liposome solution with buffer solution; compressing it via panlite film into uniform diameter, filtering out the organic solvent, to obtain blank liposome, adding alcaine solution, using pH adjuster to adjust pH value to alkali, to prepare the carrier liposome; or dissolving phosphatide, cholestrin and alcaine into organic solvent; atomizing and drying, vacuum drying or other method to remove organic solvent, to film the liposome; adding hydrating solution with drug to form carrier liposome. The inventive liposome has 50-200nm diameter and more than 95% package rate, with stable property.
US20090253696 Substituted pyrido(3,2-d) pyrimidines and pharmaceutical compositions for treating viral infections This invention provides di-, tri- and tetra-substituted pyrido(3,2-d)pyrimidine derivatives with specific substituting patterns, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular being highly active antiviral agents. The invention also provides use of such derivatives in the treatment of viral infections and pathologic conditions associated therewith, including hepatitis C.
CN1927280A Liniment for treating vitiligo and preparation method thereof The invention relates to a liniment for the treatment of leucoderma, wherein the raw materials include black soybean, black sesame seeds, flavescent sophora root, oak-apple, iron rust and abalone shell.
WO2007130383A2 Compositions and treatments using pyridazine compounds and secretases The invention relates to compositions, conjugates and methods comprising pyridazine compounds and secretase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.
CN103641871A Macrocyclic polyphenol compound, and preparation and application thereof in pharmacy The invention provides a new use of a macrocyclic polyphenol compound separated from a penthorum chinense pursh extract in pharmacy. The macrocyclic polyphenol compound comprises a compound 1, a compound 2, a compound 3 and a compound 4, wherein the structural formulas of the compounds are as shown in the specification; the compounds have the following pharmacological activities that (1) the alpha-amylase activity is significantly inhibited, and the compounds have certain hypoglycemic effects, and (2) TGF (transforming growth factor)-beta1-induced hepatic stellate cell proliferation is significantly inhibited, and the compounds have anti-liver-fibrosis effects by pharmacology and efficacy experiments. The invention provides a novel medicament for preventing and treating diabetes mellitus, and an anti-liver fibrosis medicament. The medicament is abundant in raw material source, small in side effect, and beneficial to environmental protection, and has a relatively great clinical application value.
CN103381168A Applications of Chukrasone A in antidepressant medicines The invention relates to applications of Chukrasone A in antidepressant medicines. The invention provides the applications of Chukrasone A in antidepressant medicines. Chukrasone A of the invention can be used as medicines to prevent or cure depression. The applications of Chukrasone A in antidepressant medicines of the invention are discloses for the first time. The molecular skeleton is novel, so that the antidepressant activity is surprisingly strong, and it is impossible to estimate the antidepressant activity according to the antidepressant activities of other compounds. Chukrasone A possesses outstanding substantiality, and the applications of Chukrasone A in antidepressant medicines possess significant advantages.
WO2007030166A3 TRICYCLIC 6-ALKYLIDENE-PENEMS AS CLASS-D β-LACTAMASES INHIBITORS This invention relates to certain tricyclic 6-alkylidene penems which act as a inhibitor of class-D enzymes. β-Lactamases hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. In accordance with the present invention there are provided compounds of formula I which are useful for treatment of bacterial infections having class-D enzymes associated therewith (Formula I): wherein: One of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is S or O.
US20110117036 Compositions and Methods for Improving Skin Appearance Skin conditioning compositions comprising a C4 to C30 monoalkyl-, dialkyl, monoalkanoyl- or dialkanoyl-substituted isohexide are found to exhibit a marked effect on skin hydration and barrier function homeostasis thereby improving skin appearances.
CN1839861A Effervesce tablet for dredging thrombosis and its preparation process Each of the disclosed tablet contains Notoginsen triterpenes 25-100mg, lactin 100-415mg, tartaric acid 28-120mg, stevioside 5-20mg, polyethylene glycol 6000 12-50mg, sodium hydrogen carbonate 26-110mg, and magnesium stearate 1-5mg. The preparing process consists of (1) disintegrating and mixing the raw material, making soft material with ethanol, sieving and drying, (2) heating polyethylene glycol 6000, charging sodium hydrogen carbonate, stirring, cooling down and disintegrating, sieving, mixing with the obtained particles and magnesium stearate, (3) pelleting.
CN1965812A Two kinds of tablet of cinnamyl aldehyde and preparation process thereof The invention relates to a cinnamic aldehyde slow-release tablet for treating viral myocarditis and cinnamic aldehyde mouth disintegration tablet for treating arrhythmia. The invention uses the cinnamic aldehyde which can be antiviral and stabilize heart beat. The slow-release tablet has low toxicity, antiviral property, etc. And it has simple application to be used in variable patients, etc.
WO2007115670A1 N-oxides of heterocyclic substituted bisarylureas for treating kinase-mediated diseases The present invention relates to heterocyclic substituted N-Oxides of formula (I), the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
CN103118673A Fat-reducing agent A fat-reducing agent, comprising, as an active ingredient, a carotenoid-containing composition, which comprises a carotenoid component containing at least one type of crystalline carotenoid, at least 90% by mass of the crystalline carotenoid being in an amorphous state, and also comprises a (poly)glycerin fatty acid ester having 1 to 6 glycerin units, 1 to 6 fatty acid units, and at least one glycerin unit-derived hydroxy group.
EP2026794A1 Xanthone derivative for the treatment of muscular disorders The present invention refers to compounds of the general formulae I as defined above, preferably α-mangostin, for use as/in a composition (especially foods and dietary supplements, cosmetic, as well as pharmaceutical compositions) for the prevention and improvement of muscular disorders and for the improvement of muscle function and endurance. Other fields of use are eating disorders such as bulimia and anorexia nervosa, use for accelerating wound healing, and/or use for the treatment/prevention of bone disorders such as osteoporosis and osteopenia. The present invention is also directed to dietary compositions such as (fortified) food, beverages, (fortified) feed, food additives, beverage additives, feed additives, clinical nutrition, dietary supplements, functional food, functional feed and nutraceuticals and to pharmaceutical compositions containing such compounds, to methods of preventing and/or treating the above mentioned disorders/diseases, as well as to methods of maintaining the healthy state and/or improving the baseline conditions in mammals including humans and to the compounds of the formula I themselves. Another object of the present invention is the use of such compounds for the manufacture of a composition for the prevention and/or treatment of such disorders/diseases as mentioned above.
CN102000034A S-pantoprazole sodium composite for injection and preparation method thereof The invention provides an S-pantoprazole sodium composite for injection, which is prepared through a method comprising the following steps of: (1) preparing liquid medicine: selecting S-pantoprazole sodium and edetic acid or edetate as raw materials, wherein the weight ratio of the S-pantoprazole sodium and the edetic acid or the edetate is 1:0.01-0.1; weighing a right amount of the raw materials, placing into a preparation tank, adding water for the injection till the weight of a solution is 11.82-118.2 times more than that of the S-pantoprazole sodium, stirring for dissolution, uniformly mixing, and regulating the pH value of the solution at 10.0-12.5; (2) finishing active carbon; (3) absorbing; (4) carrying out aseptic filtration and split charging; and (5) carrying out vacuum freeze drying so as to obtain the S-pantoprazole sodium composite for the injection. The S-pantoprazole sodium composite for the injection and the preparation method thereof can both ensure that product heat sources, visible foreign matters and insoluble particles meet the requirements of injections for the injections, i.e. S-pantoprazole sodium preparing liquid medicine which has higher pH.
WO2013127728A1 Hormone containing emulsion The present invention relates to a hormone containing oil-in-water emulsion for parenteral administration comprising a) progestogen and/or estrogen and b) fish oil triglycerides, wherein the fish oil triglyceride consists of glycerol which is esterified with fatty acids wherein said fatty acids comprise eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in an amount of at least 45 % by weight of said fatty acids.
CN101810623A Ceftazidime medicinal composition for injection and preparation method thereof The invention relates to a ceftazidime medicinal composition for injection and a preparation method thereof. The ceftazidime medicinal composition for injection comprises the following components in part by weight: 1 part of ceftazidime, 0.05 to 0.5 part of arginine and 0.0001 to 0.001 part of antioxidant. The ceftazidime medicinal composition for injection provided by the invention has the advantages of good dissolubility, good quality, stable color and luster and low polymer content, and the polymer content cannot be increased due to the increment of storage time, so that the medication safety is improved.
US8440220 Sustained release of drug antagonist; analgesic reservoir, barrier layer A transdermal analgesic system having reduced potential for abuse, wherein the system provides for the controlled release of the antagonist at a rate sufficient to provide an abuse limiting release rate ratio of the antagonist to the analgesic when the dosage form is subject to abuse is disclosed.
CN102250095A Carbapenem derivative or hydrate crystal and preparation method thereof The invention belongs to the technical field of medicines and particularly relates to crystal of a carbapenem derivative, namely (4R,5S,6S)-3-[(3S,5S)-5-[(4- sulfonamidophen-1-ylmethyl)aminoformyl]-3-pyrrolidyl]thio-6-[(R)-1-hydroxyethyl]-4-methyl-7-oxy-11-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, of a structural formula (I) or hydrate of carbapenem, and a preparation method thereof. When the crystal of the carbapenem derivative of structural formula (I) or hydrate of carbapenem is irradiated by Cu-Ka, a X-ray powder diffraction spectrum represented at angle of 2theta has characteristic peaks at wavelengths of 10.3+/-0.2, 14.5+/-0.2, 18.0+/-0.2, 20.8+/-0.2 and 23.3+/-0.2. The formula (I) is shown below.
DE102010053748A1 Composition, useful to treat and/or prevent obesity, comprises a specified range of hydoxycarboxylic acid, protein powder, sodium bicarbonate and magnesium carbonate Composition (I) comprises 30-80 wt.% of at least one 4-6C-hydoxycarboxylic acid, 3-20 wt.% of protein powder, 3-30 wt.% of sodium hydrogen carbonate and 5-40 wt.% of magnesium carbonate. - ACTIVITY : Anorectic. - MECHANISM OF ACTION : None given.
CN102558234A Method for preparing arsanilic acid preparation by diazotization of amino phenylarsonic acid The invention discloses a method for preparing an arsanilic acid preparation by diazotization of amino phenylarsonic acid. The method is characterized by comprising the following steps of: performing diazotization reaction on an amine salt of amino phenylarsonic acid in the presence of hydrochloric acid and sodium nitrite to generate p-amino phenylarsonic acid diazonium salt; denitrifying the p-amino phenylarsonic acid diazonium salt under the action of cuprous chloride to generate p-chlorobenzene arsenic acid; reacting the p-chlorobenzene arsenic acid with trimethoprim (TMP), removing monomolecular HCl or dimolecular HCl under the catalysis of alkali, and generating a single-substituent product or a double-substituent product simultaneously carrying p-amino phenylarsonic acid and TMP groups. The water-soluble side chain (TMP) is in covalent linkage to a water-insoluble medicament (arsanilic acid), and the arsanilic acid is converted to a water-soluble medicament, so that the defect of low bioavailability caused by low medicament solubility and poor absorption is overcome.
EP2236494A1 Sulfonyl substituted 6-membered ring derivative [Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2, Y represents CR3 or N, R1 represents a C1-6 alkyl, C3-8 cycloalkyl, etc., R2 represents phenyl or a heteroaryl, etc., R3 and R4 each independently represent a hydrogen atom, a C1-6 alkyl, etc., M1, M2, M3, and M4 each independently represent a hydrogen atom, a C1-6 alkyl, etc.]
EP1075262B1 Desmethylpantoprazole compositions and methods Methods and compositions are disclosed utilizing desmethylpantoprazole for the treatment of ulcers in humans. Desmethylpantoprazole exhibits a lessened liability toward drug-drug interactions than pantoprazole and a more predictable dosing regimen than pantoprazole. Desmethylpantoprazole is also useful for the treatment of gastroesophageal reflux and other conditions related to gastric hypersecretion such as Zollinger-Ellison Syndrome.
CN102885802A Application of lapachol to preparation of anti-human-immunodeficiency-virus-1 (HIV-1) medicine The invention relates to the application of lapachol to the preparation of an anti-human-immunodeficiency-virus-1 (HIV-1) medicine. The medicine can prevent host limiting factor BST-2 from being degraded by HIV-1 accessory protein Vpu, and improve content of BST-2 on cell surfaces, thereby preventing the liberation of HIV-1.
CN1923839A (9S)-Erythromycylamine water-soluble salt, preparation method and application thereof The invention discloses a (9S)-erycin amine soluble salt and preparing method and application in the medical, which is characterized by the following: reacting (9S)-erycin amine and medical acid with molar rate at 1: 1-2.5; reserving for a long time without crystallizing; stabilizing the quality.
CN103371993A Application of n-3 unsaturated fatty acid in preparation of medicine for preventing and treating traumatic brain injury The invention belongs to the field of medical technology, and relates to an application of n-3 unsaturated fatty acid in preparation of a medicine for preventing and treating traumatic brain injury. The experimental results about the function of n-3PUFAs (polyunsaturated fatty acids) in resisting traumatic brain injury show that the n-3 unsaturated fatty acid can remarkably improve sense and motor functions of a mice after traumatic brain injury, slightly reduces the deletion of brain tissue after injury, inhibits the inflammatory response from excessive activation, promotes the repair of white matter damage, obviously reduces the degeneration and necrosis of nerve cells of CA3 area of hippocampus, and improves the study and memory functions. The n-3PUFAs has a definite neuroprotective effect in resisting brain injury, can be used for preparing nerve protective medicines, and can be used for preventing and treating acute or chronic injury caused by the traumatic brain injury.
US20100119561 Compositions Having a Performance Indicator Compositions containing a delivery system including polymeric microparticles capable of undergoing a visual change, such as a color change, after application to a substrate are disclosed. The delivery system informs a consumer that the composition has been properly applied and/or has performed its intended function.
WO2006078283A3 Quinoxaline inhibitors of hedgehog signalling The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I wherein A is a carbocycle or heterocycle; X is alkylene, NR4C(O), NR4C(S), NR4C(NH), NR4SO, NR4SO2, NR4C(O)NH, NR4C(S)NH, C(O)NR4, C(S)NR4, C(NH)NR4, NR4PO or NR4PO(OH) wherein R4 is H or alkyl; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl or a heterocycle each of which is optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R2 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R3 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; m is 0-3; n is 0-3; and salts and solvates thereof.
CN102106978A Medicament for treating nephritis The invention discloses a medicament for treating nephritis, which is prepared from the following raw materials by weight: 1,000 grams of glucose, 4.5 grams of vitamin C, 150 grams of kidney qi pills, 60 grams of kidney boost tables, 500 milliliters of artificial hematinic liquid, 100 grams of corn stigma, 15 Chinese dates and 4.2 kilograms of water, and the components are prepared into oral liquid by the conventional method. The medicament has the effects of tonifying qi, promoting blood circulation, tonifying liver and kidney, supplying vital essence and marrow and enhancing the immunity oforganisms, has the effect of curing and rehabilitating kidney diseases, is non-toxic and harmless to human bodies, and is not bitter nor astringent and convenient to take. Cases are selected during years of clinical observation, one month is one treatment course, the medicament is taken for three times a day, and one bottle is taken at each time; about 500 patients are cured, cure means the patients are rehabilitated completely, and effectiveness means the condition of the patients has a favorable turn; and the cure rate is 85 percent, and the total effective rate is 95 percent.
CN102309766A Method for improving water solubility of xanthohumol The invention relates to a method for improving water solubility of xanthohumol, belonging to the field of fine chemical industry. The method comprises the following steps: dissolving xanthohumol and cyclodextrin in diluted alcohol; recovering alcohol by reduced-pressure distillation; filtering to obtain an aqueous solution of a cyclodextrin-xanthohumol clathrate compound; and drying to obtain a cyclodextrin-xanthohumol clathrate compound powder product. By the method provided by the invention, the water solubility of xanthohumol is improved, and the solubility of the formed cyclodextrin-xanthohumol clathrate compound in water at the room temperature is more than 10%, thereby creating conditions for wide application of xanthohumol.
EP2407161A1 An antitumoral combination comprising ombrabulin and bevacizumab The invention concerns an antitumoral combination comprising ombrabulin and bevacizumab, and its use in the treatment of advanced solid tumors.
CN103110598A Alfacalcidol dispersible tablet and preparation method thereof The invention discloses an alfacalcidol dispersible tablet and a preparation method of the alfacalcidol dispersible tablet. The alfacalcidol dispersible tablet is prepared from an alfacalcidol clathrate compound and a preparation supplementary material, wherein the preparation supplementary material comprises a filling agent, a disintegrating agent, a diluting agent, a lubricating agent, a flow aid and a flavouring agent; and the alfacalcidol clathrate compound is prepared by carrying out clathration on alfacalcidol and 2,6-dimethyl-Beta-cyclodextrin based on the molar ratio of 4: 1 to 0.5: 3. The alfacalcidol dispersible tablet has the advantages of being quick to dissolve out, fast to absorb, high in bioavailability, excellent in stability, convenient to take, etc.
EP1900365A2 New endocannabinoid-like compounds and their use The present invention describes compounds deriving from chemical reactions between saturated or monounsaturated acyl derivatives and primary amines or primary alcohols that display specific cannabinoid-like pharmacological activity without exhibiting the central unwanted side effects typical of synthetic cannabinoids or endocannabinoids acting on central cannabinoid (CB1) receptors. These compounds, having this pharmacological activity, may be utilised to prevent or to treat pathological conditions and diseases in mammals, including human subjects, that may undergo a clinical improvement upon their administration.
CN101698009A Externally-applied medicament for treating skin diseases The invention relates to an externally-applied medicament for treating skin diseases. The medicament can be used to treat various suppurative skin diseases, sycosis, empyrosis and external hemorrhoid, and can also be used to prevent corrosion of skin wound surface. The medicament comprises the following raw materials in part by weight: 15-40 parts of coptis, 15-35 parts of pearl, 15-30 parts of borneol and 100-200 parts of Vaseline. The medicament has no toxic and side effect and no scar after the wound is healed; and the medicament is an ideal externally-applied medicament for treating various suppurative skin diseases.
US20070225311 Condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence; selective cytotoxic activity on human tumor cell lines; antitumor; Compounds of Formula (I) are described: in which the R1 group is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
WO2012071414A2 Quinoxaline compounds and uses thereof Disclosed herein are compounds of formula (I) and methods of inhibiting ΙΚΚβ and the NF-κB signaling and mTOR pathways.
CN103478522A Donkey-hide gelatin and propolis soft capsules and preparation method thereof The invention discloses donkey-hide gelatin and propolis soft capsules and a preparation method thereof, and belongs to a health-care product and a preparation method thereof, in particular to soft capsules using donkey-hide gelatin and propolis as main raw materials and a preparation method thereof. The soft capsules are characterized by being prepared from the following raw materials in parts by weight: 35 parts of donkey-hide gelatin, 10 parts of propolis, 5 parts of lycopene, 5 parts of grape seed extract OPC (oligomeric proanthocyanidins), 44 parts of salad oil and 1 part of vitamin E which are used as inclusions, and gelatin and glycerin which are used as shell materials. The donkey-hide gelatin and the propolis in the soft capsules have the effects of regulating body immunity, regulating blood fat, delaying senescence, maintaining beauty and keeping youth, and the compatibility effect of the donkey-hide gelatin and the propolis is obviously higher than the single curative effect of any of the both. The OPC and the lycopene substitute a large dose of vitamin E in donkey-hide gelatin soft capsules and propolis soft capsules, so as to greatly enhance single anti-oxidation and immunity promoting effects of the both.
WO2011127070A2 IRE-1α INHIBITORS Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
CN101732242A L-ornidazole sodium chloride injection L-ornidazole sodium chloride injection is mainly characterized in that: (1) L-ornidazole belongs to third-generation azomycin and plays an antimicrobial role in causing the death of microorganisms through the reduction of nitro-groups in molecules into amino groups in an oxygen-free environment or through the formation of free radicals and coaction of cell constituents; and the L-ornidazole sodium chloride injection is also characterized by: (2) wide antimicrobial spectrum: the injection plays a strong role in killing almost all pathogenic anaerobic bacteria and protozoans, such as infusorium, amoebas and giardia lamblia; (3) strong sterilizing power: ED90 for various sensitive pathogens is lower than metronidazole; (4) good clinical efficacy: the solution has higher effective rate and curative ratio on anaerobic bacteria and infusorium than those of like products; (5) high safety: no teratogenesis or carcinogenesis or mutagenesis effect is found in the solution; and (6) good tolerance: the overall adverse reaction rate of the solution is lower than that of the like products.
EP1899325B1 Imidazolinone and hydantoine derivatives as novel inhibitors of histone deacetylase This invention comprises the novel compounds of Formula (I) wherein R1, R2, R3, X, Y and Z have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
CN101553238A Compositions for providing hepatoprotective effect This invention relates to a composition for injection comprising a neutral polysaccharide of Antrodia camphorata having characteristics as follows: (a) appearance: colorless and shapeless powder, (b) pH: neutral, (c) molecular weight: 899.5-1670.5 kDa determined by HPLC as shown in (4), (d) rotatory power: (alpha)D+115.0 degree (c=0.4433, H2O), (e) intrinsic viscosity: (eta)=0.03971-0.06255 dl.g, (f) specific heat Cp: 0.2536-0.3995 Cal/g.DEG C, (g) IR spectrum: as shown in (5), (h) H-NMR spectrum: as shown in (6), (i) C-NMR spectrum: as shown in (7), and (j) GC-MS analysis: as shown in (8). This invention also relates to a composition for oral administering comprising a neutral polysaccharide of Antrodia camphorata having characteristics (a)-(j) as above.
WO2013153394A1 Quinolonones with antibacterial properties This invention relates to derivatives of fluoroquinolone antibacterial drug compounds. It also relates to pharmaceutical formulations of derivatives of fluoroquinolone antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections and in methods of treating bacterial infections.
WO2005030192A1 4- (1h-indol-3-yl-methylideneaminoxy-propoxy) -benzioc acid derivatives and related compounds as pai-1 inhibitors for the treatment of impairment of the fibrinolytic system and of thrombisis The present invention relates to substituted indole oximes and methods of using them.
CN101601663A Multi-unit sustained-release preparation of levetiracetam and preparation method thereof The invention discloses a multi-unit sustained-release preparation of levetiracetam and a preparation method thereof, wherein the preparation is prepared by filling a plurality of independent sustained-release unit bodies with pharmacological activity into capsules. The sustained-release unit bodies consists of medicament carrying core bodies containing levetiracetam active components and coating layers enwrapped outside the medicament carrying core bodies, and the sustained-release unit bodies can also are prepared by adding a retardant material for retarding the medicament release into the medicament carrying core bodies, or adding a functional coating material for prolonging the medicament release time into the coating layers, or adopting the combination of the two modes. The multi-unit sustained-release preparation of the levetiracetam is released slowly, stably and uniformly in vivo due to the unique formulation and preparation method thereof, has no medicament burst release phenomena and is not influenced by foods so that the blood-medicament concentration is more smooth, the time for the medicament to take effect is longer, the untoward effect is obviously lightened, and the compliance of patients is greatly improved, thus the multi-unit sustained-release preparation of the levetiracetam is a novel and high-efficiency anti-epileptic pharmaceutical preparation.
US20090030028 Tetrahydroquinolines Disclosed are compounds of formula (I), wherein W, R, R1, R2, R3, R4, R5, R6, and R7 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.
US7122173 A compound having slowly-deactivating A-type K+ channel opening activity such as N-(5,5-dioxido-10-oxo-4,10-dihydrothieno[3,2-c][1]benzothiepin-9-yl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide The present invention provides an agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising, as an active ingredient, a compound having a slowly-inactivating A-type K+ channel opening activity or a pharmaceutically acceptable salt thereof, and a method for screening agents for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising measuring a slowly-inactivating A-type K+ channel opening activity as an index.
WO2014027882A1 Product and method for supporting uridine homeostasis This invention pertains to the use of an uridine source, preferably uridine monophosphate,for increasing, controlling and/or maintaining fasting plasma uridine concentrations in a range of 4 to 8 µM in a subject in need thereof, comprising administering to said subject a composition comprising 300 –900 mg of said uridine source daily for a period of at least 4 weeks. In particular, the use of an uridine source is intended forelderly and/or subjects suffering from neurological disorders such as Alzheimer's Disease and dementia syndromes.
CN101766672B Composition for anti-alcohol and sobering The invention discloses a composite (D) for disintoxicating and sobering, which is prepared by glucose and fructose, fruit glucose, honey, root of kudzuvine, flower of kudzuvine, L-alanine, L-ornithine, L-glutamine, L-carnitine according to a certain weight range. In order to enable the effect better, one or more of tea leaf, vitamin C, L-cysteine, taurine, L-asparaginic acid or L-aspartate, vitamin B1, vitamin B6, L-arginine, L-glutamic acid, L-proline, phaseomannite, vitamin B2, nicotinic acid, folic acid, vitamin B12 and pantothenic acid are also added. The composite can be prepared into liquid preparation, electuary and medicinal tea. The composite of the invention can be prepared into food and health food. The invention can quickly disintoxicate, sober, eliminate alcoholism symptom and continued effect of alcohol on a human body, and has no side effect.
US20100135960 Antiviral acylsulfonamide derivatives The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
US20080095754 Epithelium cell stabilizer component comprising diglycine, triglycine, tetraglycine and/or pentaglycine for use in treatment of dry eye An ophthalmic composition that includes an epithelium cell stabilizer component. The epithelium cell stabilizer component may be one or more of diglycine, triglycine, tetraglycine, pentaglycine. The invention is also directed to a method of treating or preventing dry eye comprising administering an effective amount of the ophthalmic composition to the eye.
US20080070962 Cannabinoid receptor antagonist; N-{[5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-1H-pyrazol-3-yl]methyl}-3-cyanobenzenesulfonamide; psychiatric disorder, substance dependence and withdrawal disorder, cognitive disorder, ADD, neurodegenerative diseases, pain, eating disorders, dyslipidemia, ulcer The present invention relates to compounds corresponding to the formula (I): In which R1, R2, R3, R4 and R5 are as described herein. The invention also relates to the method of preparation of said compounds and their application in therapeutics.
WO2008095689A1 Heterocyclyl substituted tetrahydronaphthalene derivatives as 5-ht7 receptor ligands The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen compounds of general formula (I) and (I prot), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals, mediated by the receptor 5-HT7 affinity.
WO2007002325A1 Pyrrolo[2,3-b] pyridine derivatives as protein kinase inhibitors Compounds of formula III which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
CN102232953A Medicinal composition containing Esopiclone and preparation method thereof The invention discloses a medicinal composition containing Esopiclone and a preparation method thereof. The Esopiclone-containing medicinal composition consists of a main medicine and auxiliary materials. In the invention, by controlling the particle size of the main medicine, a pre-mixing method and the auxiliary materials, the medicinal composition which has high dissolution rate and high content uniformity can be obtained. The preparation method adopts a modern preparation technique, the quality of the product is stable, and an Esopiclone-containing solid oral preparation which is safe, effective, quick in absorption, high in bioavailability and accurate in dosage is provided for patients.
US20090042828 Nucleic acid with 1st sequence encoding antisense RNAi specific for targeting regions of copper zinc superoxide dismutase that cause inherited amyotrophic lateral sclerosis, and a 2nd sequence encoding a RNAi resistant replacement gene with silent mutations encoding messenger RNA resistant to cleavage The present invention relates to novel methods for treating dominant gain-of-function diseases. The invention provides methods for targeting regions of the copper zinc superoxide dismutase (SOD1), which causes inherited amyotrophic lateral sclerosis (ALS), with RNAi agent. The invention further provides RNAi resistant replacement genes containing mismatches with their respective RNAi agents. The invention also provides for vectors that express RNAi agent and RNAi resistant replacement gene of the present invention.
US7851622 6-(4-Chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-thieno[3,2-d][1,2,3]triazin-4(3H)-one, for example; for treating a patient suffering from an MCHR-1 modulated disease or disorder such as obesity, diabetes, depression or anxiety The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I where R1, R1a, R1b, A, R3, R4, R5, R5b and R6 are as defined herein.
US20090060889 Ii-RNAi involved Ii suppression in cancer immunotherapy Provided are compositions and methods involving the inhibition of Ii expression in cells for the purpose of altering antigen presentation pathways. Human Ii-RNAi constructs that effectively inhibit Ii expression in human cancer cells have been generated. The combination of different Ii-RNAi constructs that target different positions of Ii mRNA has a synergistic effect on Ii inhibition. Furthermore, specific promoters for driving Ii-RNAi expression are critical for the activity of Ii-RNAi in different types of cells. Active Ii-RNAi sequences were cloned into plasmids in which Ii-RNAi sequences are driven by either a CMV or an EF-1α promoter. Compositions and methods are disclosed for inhibiting Ii and treating cancer. Provided are siRNAs and expression constructs comprising DNA sequences which encode siRNAs effective to inhibit Ii expression, cells containing such DNA constructs or siRNAs, and methods for use of the same.
CN102342910B Levofloxacin hydrochloride injection pharmaceutical composition and preparation method thereof The invention discloses a levofloxacin hydrochloride injection pharmaceutical composition and a preparation method thereof. The preparation method comprises the following steps of: dissolving levofloxacin hydrochloride with a proper amount of water for injection, adding a prescription amount of vitamin B6, lipoic acid and 2.3 g of activated carbon, then adding water for injection to 1000 ml, decarbonizing and filtering, detecting the intermediate, filling, performing moist heat sterilization at the temperature of 121 DEG C for 20 minutes, carrying out leakage detection and lamp inspection, and packaging a finished product. The levofloxacin hydrochloride injection pharmaceutical composition and the preparation method thereof have the advantages that: the characteristic that vitamin B6 is easy to damage under illumination is utilized to cover up the damage caused by illumination on levofloxacin hydrochloride in the production process; lipoic acid is used as an antioxidant and metal chelating agent, thereby reducing the oxidation loss of levofloxacin hydrochloride and reducing the generation of insoluble complex due to complexing of levofloxacin hydrochloride and multivalent metal introduced in the production process; and because the damage caused by metal element, illumination and high-temperature sterilization on the product are reduced, the total amount of insoluble microparticles in the finished product of a new combined formula drug is reduced, the color of the product is lightened, and the ratio of related substances is reduced.
WO2009080030A1 Treatment of autoimmune hepatitis with a once daily oral dosage form comprising tacrolimus Treatment of autoimmune hepatitis with an extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily treatment of a patient in need thereof. The dosage form releases the active substance over an extended period of time defined by a release of at the most 63.5% of the content of the active substance at the 12 hours time point defined by in vitro dissolution and when tested according to the USP Il dissolution test (paddle) or USP I dissolution test (basket) form in a medium at pH 4.5 and comprising 0.005% hydroxypropylcellulose and a rotation of 50 rpm. The extended release dosage form provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release dosage form. The treatment further provides for reducing the dosage of steroids compared with the dosage needed for a conventional treatment of autoimmune hepatitis such as with azathioprine.
WO2010001926A1 Water-containing composition When a poorly water-soluble ultraviolet ray absorber is used, it is difficult to solubilize a sufficient amount of the poorly water-soluble ultraviolet ray absorber by using a surfactant such as a polyoxyethylene alkyl ether or a polyoxyethylene hydrogenated castor oil. Thus, an object aims to provide a water-containing composition in which a poorly water-soluble ultraviolet ray absorber is solubilized or dispersed in water. Another object aims to dissolve a poorly water-soluble ultraviolet ray absorber in water and allow the poorly water-soluble ultraviolet ray absorber to co-exist with a water-soluble component such as a water-soluble medicinal agent and a water-soluble dye in the water to thereby stabilize the water-soluble component. The water-containing composition comprises the components (1) to (3) shown below and may additionally comprise a water-soluble medicinal agent and/or a water-soluble dye: (1) a polyoxyethylene adduct compound represented by formula (I) HO(CH2CH2O)n-R (I) [wherein R represents a phytosterol residue or a phytostanol residue; and n represents a number of 5 to 100]; (2) a poorly water-soluble ultraviolet ray absorber; and (3) water.
CN103524555A Rhein aminophosphonate derivatives, and synthetic method and applications thereof The invention discloses a series of rhein aminophosphonate derivatives, and a synthetic method and applications thereof. The synthetic method of the rhein aminophosphonate derivatives comprises: taking rhein and an alpha-aminophosphonate as raw materials, dissolving in a polar solvent, in the presence of a catalyst HOBT and a condensing agent EDAC, reacting completely; and adding trichloromethane into the reaction liquid, washing with water, collecting the organic layer, applying to silica gel for column chromatography, eluting with a mixed solvent of ethyl acetate and petroleum ether with a volume ratio of 1:4-100 to obtain the corresponding derivative. The rhein aminophosphonate derivatives have the structural general formula (I) as shown in the description, wherein R is p-bromophenyl, o-bromophenyl, m-bromophenyl, p-fluorophenyl, o-fluorophenyl, p-chlorophenyl, m-chlorophenyl, o-chlorophenyl, m-methoxyphenyl, o-methoxyphenyl, phenyl, naphthyl, p-methoxyphenyl, m-methylphenyl, p-methylphenyl, m-fluorophenyl or anthryl.
WO2008023998A1 N-acylethanolamines as wound healing agents The use of compounds for promoting the healing of wounds, having the formula 1: where R is a straight or branched chain C1-C30 alkyl which may be substituted by one or more hydroxyl groups or halogen atoms, and may contain one or more epoxy groups. The wounds treatable include chronic wounds, such as cuts, scratches, abrasions, oral ulcers, stomach ulcers, ulcers from cancer therapy, diabetic foot ulcers, venous stasis ulcers, pressure ulcers, and burns, as well as wounds that result from ophthalmic surgery, cosmetic surgery, general surgery, treatment for keloids and hypertrophic scars (anti-scarring treatments).
WO2006021441A1 Biphenyl-carboxylic acids and derivatives thereof and their use in therapy The present invention relates to compounds having the general formula (I) with the definitions of R1-R4 given below, and/or salt or ester thereof. Furthermore, the invention relates to the use of said compounds as a medicament, preferably for the treatment of Alzheimer's disease and their use for the modulation of Ϝ-secretase activity.
US20050153315 Nucleotide sequences coding polypeptide comprising methylarginase activities for use in identifying modulator for prevention and treatment of ischemia-reperfusion injuries, cancer, hypotension, multi-organ failure, arthritis, skin, inflammatory, cardiac and/or migraine disorders Two dimethylarginine dimethylaminohydrolase (DDAH) genes have been cloned from humans. These genes can be used to screen for inhibitors and activators of activity and/or expression of DDAHs. Inhibitors and activators of activity and/or expression of DDAHs are useful in the treatment of conditions in which abnormal metabolism of nitric oxide is implicated.
EP1461032B1 Use of c-kit inhibitors for promoting hair growth The present invention relates to a method for promoting hair growth, preventing or minimizing hair loss comprising administering a tyrosine kinase inhibitor to a human in a need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.
US20080221014 Method of Diagnosing and Treating Glioma The present invention is directed to methods and compositions for the diagnosis, prognosis and treatment of glioma in mammals.
US20100324034 Methods of Using SAHA for Treating HIV Infection The present invention relates to pharmaceutical preparations and methods for treating individuals infected with the human immunodeficiency virus (HIV). The pharmaceutical preparations comprise SAHA and another anti-viral agent. The invention also relates to methods for treating HIV infected patients, particularly patients with persistent, latent HIV infection of CD4+ T cells, and thus make it possible to not just suppress but to eradicate the HIV infection.
US20090137627 Method for Treating Chronic Pain A method for the treatment of chronic pain in a mammal is provided. The method comprises administering to a mammal (e.g., a human) suffering from chronic pain a pain relieving amount of a diarylureido-dihalokynurenate compound. Preferred diarylureido-dihalokynurenate compounds are esters (e.g., ethyl esters). Particularly preferred are diphenylureido-dichlorokynurenate compounds.
CN102058615B Novel pharmaceutical application of Lachnum calyculiforme polysaccharides The invention discloses a pharmaceutical application of Lachnum calyculiforme polysaccharides in preparing antifatigue medicaments. Pharmacodynamic tests prove that the purified Lachnum calyculiforme polysaccharides can distinctly prolong the mice burden swimming time, greatly increase the contents of mouse hepatic glycogen and muscle glycogen, increase the activity of serum lactate dehydrogenase, and remarkably reduce the content of blood urea nitrogen of mice after strenuous exercises; and the Lachnum calyculiforme polysaccharides has effects of enhancing athletic stamina and relieving physical fatigue. Therefore, the Lachnum calyculiforme polysaccharides can be used for preparing antifatigue medicaments. The Lachnum calyculiforme polysaccharides have no toxic and side effects, can be prepared into various dosage forms, and are convenient in administration.
EP1230235B1 Compounds with antibacterial and antiparasitic properties There are provided novel compounds which have both antibacterial and antiparasitic properties, thereby reducing the need for using several compounds in combined antibacterial and antiparasitic treatment of livestock. The present novel compounds are especially well suited for treatment of coccidiosis, and they are represented by general formula (I) wherein R1-R6, X and A are as defined in the specification.
CN101829064A Dexibuprofen particle and preparation method thereof The invention discloses a dexibuprofen particle which is mainly prepared from the following raw materials in parts by weight: 1-10 parts of dexibuprofen, 1-6 parts of sodium carbonate, 1-35 parts of sucrose, 0.1-0.8 part of aspartame and 3-12 parts of ethanol. The invention also discloses a preparation method of the dexibuprofen particle, which comprises the following steps of: sieving each raw material, and then, fully mixing the raw materials uniformly; granulating; and drying at high temperature, and then, refining to obtain the dexibuprofen particle. The dexibuprofen particle of the invention can endure high-temperature drying, has qualified indexes of microbial limit, solubility and the like and has stable and controllable quality; in addition, the preparation method is simple to operate has short production cycle and low cost, and is suitable for industrialized production.
EP2097390A1 Amino quinazolines derivatives wuth blood platelet reducing properties This invention relates to the discovery of prodrugs of 3-or 5-substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelet.
CN102847111A Tongli heat purging capsule The invention discloses a Tongli heat purging capsule. The capsule is characterized in that the capsule comprises Divaricate Saposhnikovia Root, Ligusticum wallichii, Chinese angelica, white peony root, fried rheum officinale, mint, Herbal Ephedrae, Weeping Forsythia, gypsum, Radix Scutellariae, Radix Platycodonis, ginger, fried licorice, Herba Schizonepetae, Rhizoma Atractylodis Macrocephalae and cape jasmine.
US7501516 3-Cyanoquinolines 4-substituted by a methylenedioxyphenyl group that is attached by a methylene, oxy, thio, sulfinyl, sulfonyl or amino group; antitumor agents The invention concerns quinoline derivatives of Formula (I) wherein each of Z, m, R1, n and R3 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
CN103599093A Novel anti-HPV (Human Papillomavirus) medicinal preparation and application The invention discloses a novel anti-HPV (Human Papillomavirus) medicinal preparation and application. Each unit dose of the anti-HPV medicinal preparation contains 1-500 mg of acetaminophen, and is the total amount of the medicinal preparation used each day. In the medicinal preparation, acetaminophen can be combined with other medicines or used independently; a pharmaceutically acceptable medicinal carrier is added to prepare any clinically acceptable formulation, wherein acetaminophen accounts for 0.1-40 percent of the total weight of the medicinal preparation. The invention also provides application of acetaminophen and the acetaminophen-containing medicinal preparation to preparation of the anti-HPV medicaments. The novel anti-HPV medicinal preparation has the characteristics of simple preparation method, low production cost, obvious anti-HPV effect and low toxicity, can be used for preventing and treating clinical symptoms caused by HPV infection, and is particularly suitable for verruca vulgaris, flat wart, plantar wart, carcinoma of vulva, carcinoma of penis, anal epidermoid cancer, prostatic cancer, carcinoma of urinary bladder, cervical cancer, rectal cancer, oral cancer, carcinoma of tonsil and the like.
EP1359909B1 Triptolide prodrugs for anti-cancer therapy Water soluble triptolide prodrugs are used as anticancer agents, and are found to be more effective in vivo, at lower doses, in reducing tumor size than the widely used chemotherapeutic agents 5-fluorouracil and irinotecan.
CN101511832A Fused heterocyclic inhibitors of D-amino acid oxidase This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. Also provided are methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure wherein Q is a member selected from O, S, CR and N, X and Y are members independently selected from CR, O, S, N and NR.
EP1472259B1 Tetrapyrrolic macrocycles as photodynamic agents The invention refers to macrocyclic tetrapirrolic compounds of the family of porphyrins (structure I), chlorins (structure II) and bacteriochlorins (structure III) characterized by the presence of hydrogen or halogen atoms and/or phenyl groups with halogens in the ortho position (with or without hydroxyl groups in the meta position) in positions 5,10,15 and 20 of the macrocycle, and hydrogen or halogen atoms or akyl, vinyl, carboxy, carboxyalkyl, alkoxycarbonyl, alkoxycetoalkyl, alcoxycetoaryl, acetoxy or hydroxyalkyl groups in positions 2,3,7,8,12,13,17 and/or 18.
CN103656593A Externally-applied medicine paste for treating burns and preparation method of paste The invention discloses externally-applied medicine paste for treating burns and a preparation method of the paste. The paste comprises raw materials in parts by weight as follows: 10-15 parts of lithospermum, 5-10 parts of sanguisorba officinalis, 15-20 parts of phellodendron barks, 10-15 parts of pomegranate barks, 5-10 parts of Chinese teasel roots, 8-12 parts of rose myrtle roots, 14-18 parts of bletilla striata, 10-15 parts of fresh ginger, 5-10 parts of folium callicarpae pedunculatae, 10-15 parts of gallnut, 5-10 parts of dragon's blood, 12-16 parts of leaf of Chinese Loropetalum, 4-8 parts of ossa draconis, 8-12 parts of angelica sinensis, 10-15 parts of red-rooted salvia roots, 5-10 parts of lalang grass rhizome, 6-11 parts of boenninghausenia albiflora, 10-15 parts of frankincense, 5-10 parts of myrrh, 10-15 parts of scutellaria baicalensis, 8-12 parts of cutch, 5-10 parts of lumbricus, 14-18 parts of coptis chinensis, 5-10 parts of borneol, 8-12 parts of gypsum rubrum powder and 10-15 parts of badger fat. The externally-applied medicine paste has functions of clearing heat, cooling blood, removing necrotic tissue, promoting granulation, converging, eliminating dampness, resisting bacteria and inflammation, relieving swelling and pain, promoting blood circulation, dispersing blood stasis and the like and is capable of drying wound surfaces quickly, inhibiting bacterial growth and proliferation, shortening wound healing periods and avoiding scars after recovery, fast in recovery, significant and quick in curative effect, short in treatment course, free from side effects, low in cost, simple in technology and worthy of clinical popularization and application.
CN1651466A Sulphatization derivative of polysaccharide, its preparation method and use A polyose (YCP) sulfate derivative used for preparing anticoagulant, antithrombolic, antioxidizing medicine, antineoplastic medicine and anti-AIDS disease, and its preparing process are disclosed.
EP1392320B1 17-METHYLENE-ANDROSTAN-3a-OL ANALOGS AS CRH INHIBITORS 17-Methylene-androstan-3α-ol analogs are useful as corticotropin releasing hormone (CRH) inhibitors, and especially as anti-depressants, when administered to the vomeronasal organ. An improved synthesis of 17-methyleneandrost-4-en-3α-ol is disclosed.
WO2005004865A1 Use of 5-ht4(a)-serotonin receptor agonists This invention pertains to the use of a 5-HT4(a)-serotonin agonist or a pharmaceutically acceptable salt or ester thereof for the preparation of a pharmaceutical composition for treating or preventing drug induced respiratory depression.
US7161002 Compounds as antiinflammartory agents, antiproliferation agents and and anticancer agents from cyclodehydration of compounds The present invention provides novel quinazolinone compositions of matter comprising enantiomerically pure compound represented by Formula I: or a pharmaceutically acceptable salt thereof, having a detectable amount of one or more starting material and/or reagent used in the synthesis thereof.
US20090155374 Bioactive agent, a low molecular weight chitosan, and a negatively charged third component; the chitosan dominates on the nanoparticle surface; enhanced permeability for paracellular drug delivery; chewable composition The invention discloses the nanoparticles composed of chitosan, poly-glutamic acid, and at least one protein drug or bioactive agent characterized with a positive surface charge and their enhanced permeability for paracellular protein drug and bioactive agent delivery.
WO2009055864A1 Methods and compositions for regulating airway tissue remodelling Provided herein are methods and compositions for regulating airway tissue remodelling and for treating or preventing conditions associated with airway inflammation and/or airway tissue remodelling. The methods comprise normalising fibulin-1 levels in said tissue relative to normal endogenous levels. In an embodiment the methods comprise administering to a subject in need thereof an effective amount of at least one agent capable of inhibiting the expression and/or activity of fibulin-1.
US7632951 Inhibitors of integrin ανβ6 Novel biphenyl derivatives of the general formula (I) in which R1, R1′, R1″, R2, R2′, R3 and n are as defined in claim 1, their stereoisomers and their physiologically acceptable salts or solvates are novel integrin inhibitors which preferentially inhibit the αvβ6 integrin receptor. The novel compounds can be used, in particular, as medicaments.
CN103070830A Production method for 20-percent tilmicosin granules A production method for 20-percent tilmicosin granules comprises the following specific steps: firstly, uniformly mixing 25 kg of tilmicosin with part of 40 kg of 30-50 percent by weight of microcrystalline cellulose and 2-8 kg of vitamin B6 to obtain a mixture; secondly, mixing the mixture obtained in the first step with 15-35 kg of fused insectwax for granulating and passing through a sieve with 24 meshes to obtain granules; and thirdly, uniformly mixing the granules obtained in the second step with residual 50-70 percent by weight of microcrystalline cellulose, uniformly mixing the mixture with 10-20 kg of polyethylene glycol 4000 or 6000 in a fusion state for granulating and passing a sieve with 20 meshes to obtain a finished product. According to the product prepared by the production method disclosed by the invention, high dispersion of medicaments is ensured, the dissolving speed is increased, the solubility is increased, the sensitivity of bacteria to the product is effectively enhanced and the biological availability of organism is greatly increased.
WO2013098374A1 1,3-diphenylpropane derivatives, preparations and uses thereof The present invention relates to novel 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising the same and therapeutic uses thereof, in particular in the fields of human and animal health. The compounds according to the present invention have intrinsic PPAR agonist properties. They are therefore of particular interest in the treatment of metabolic and/or inflammatory diseases and particularly peripheral and central diseases associated with the metabolic syndrome, such as diverse forms of steatohepatitis, type 2 diabetes, diverse neurodegenerative disorders,such as Alzheimer'sdisease, Parkinson's disease and multiple sclerosis.
WO2008062044A1 2-hydroxy-1,3-diaminopropane derivatives The invention relates to novel cyclic compounds of the formula (I), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
CN101199818A Medicament compound for treating calculus The invention discloses a drug compound for treating calculi, containing 30 crude drugs such as loosestrife herb, clematis root, oxhorn filament, Endothelium Corneum Gigeriae Galli, Folium Pyrrosiae, talc and so on. The invention of the drug compound can be prepared into any dosage forms that can be accepted clinically by adding conventional excipients to the conventional technique. The invention of the drug compound is provided with the efficacies of clearing heat and secreting bile, melting and dissolving the calculus and eliminating calculus, so that lithiasis can be treated without the operation or the laser treatment and the curative effect is notable.
CN102228681A Fish spawning inducer and spawning induction method The invention discloses a fish spawning inducer. Every 1ml of spawning inducer comprises 120-200 IU (International Unit) of chorionic gonadotropin, 0.6-1.6mg of domperidone and 1.0-3.0mg of luteotropin releasing hormone d-ala analog. In the spawning induction method using the fish spawning inducer, the fish spawning inducer is injected for a female fish twice by using a pectoral fin injection method, wherein the injection dosage is as follows: 5ml of fish spawning inducer is injected for every kilogram of fish, 10-40 percent of the total dosage of the fish spawning inducer to be injected is injected for the first time, and the remaining dosage of the fish spawning inducer is injected for the second time; the injection dosage of the male fish is as follows: 2.5ml of fish spawning inducer is injected for every kilogram of fish; and the total dosage of the fish spawning inducer to be injected is injected for the male fish by using the pectoral fin injection method. By adopting the technical scheme, artificial spawning induction of parents of the Chinese fat minnow is realized, so that the spawning induction rate of the Chinese fat minnow reaches over 85 percent; the fish spawning inducer is low in cost; the spawning induction method is easy and convenient to operate; and the technical scheme has an obvious effect and is easy to popularize.
US20110313049 Antibacterial compositions comprising quaternary ammonium germicides and alkamine oxides having reduced irritation potential Antibacterial compositions having antibacterial effectiveness and reduced eye irritation potential are disclosed. The antibacterial compositions contain a quaternary ammonium compound, an alkamine oxide, a nonionic compound, optional adjuvant materials known in the art, and water. The eye irritation is decreased by decreasing the amount, by weight, of alkamine oxide present in the composition and alternatively, or in combination therewith, increasing the ratio of nonionic material to alkamine oxide present in the composition.
US7351719 Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds The present invention relates to amide compounds of general formula I wherein the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one amide according to the invention. In view of the MCH receptor-antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
US20120288571 Antimicrobial Agents and Methods of Use The present application relates to novel antimicrobial compositions and methods of using said antimicrobial compositions for inhibiting and treating microbial growth, microbial infections, inflammatory diseases, viral diseases, cardiovascular diseases, diabetes and/or conditions that may be regulated or associated with microbial infections, such as cancer.
WO2013051672A1 Medicinal agent comprising thiazolidine derivative or salt thereof as active ingredient Provided is a compound having an excellent Pim inhibition activity and useful as a medicinal agent. A thiazolidine derivative represented by general formula (1) (wherein X represents O, S or NH; R3 represents a hydrogen atom or an alkyl group; at least one of the dotted lines is a double bond; Z1, Z2 and Z6 independently represent C, CH or N; Z3, Z4, Z5, Z7 and Z8 independently represent C, CH, N, NH, O or S; Y represents a bivalent hydrocarbon group which has at least one C6-14 aromatic hydrocarbon group and may have a substituent, a bivalent aromatic heterocyclic group which may have a substituent, or a bivalent C2-12 aliphatic hydrocarbon group; Am represents an amino group, a mono-substituted amino group, a di-substituted amino group, or a nitrogenated saturated heterocyclic group which may have a substituent; and R1 and R2 independently represent a hydrogen atom, a halogen atom, an alkoxy group, a halogenoalkoxy group, or the like) or a salt thereof.
WO2014049619A1 Cancer chemotherapeutic agent/formulation, manufacture and use thereof A cancer chemotherapeutic agent that is particularly kinase suppressing and/ or any other signaling pathway interfering agents and pharmaceutical formulations/ compositions involving the same and its process of manufacture is provided. A potential the cancer chemotherapeutic agent is provided which apart from stated anticancer activity as a proven kinase suppressing and/ or any other signaling pathway interfering agent could also involve specific potential binding affinity towards the intramolecular G-Quadruplex DNA structure and/ or other potential quadruplex forming sequences over duplex DNA structures favours further diverse end use and application including but not limited to antiaging, antiangiogenic, antiproliferative, antitumor, antibiotic, antiviral, antifungal and multiple anticancer therapeutics, and also possesses favourable cytotoxicity values towards uncontrollably proliferative cells by inducing apoptosis irrespective of cells' p53 status, without being cytotoxic to normal cells.
CN103006699A Compound medicament with double effects of alleviating pain and inhibiting bacteria The invention discloses a compound medicament with double effects of alleviating pain and inhibiting bacteria. The compound medicament comprises a pharmaceutically acceptable carrier, silver powder and a pain alleviating medicament selected from lidocaine, tetracaine, prilocaine or benzocaine, wherein the weight ratio of the silver powder to the pain alleviating medicament is 1:1-1:20. The compound medicament is good in transdermal absorption, has the characteristics of broad-spectrum bactericidal effect and medicament tolerance prevention, and can reduce clinical medication times and facilitate medication of patients.
EP1599204A2 Selective mglu5 antagonists for treatment of neuromuscular dysfunction of the lower urinary tract Antagonists that are selective for the metabotropic mGlu5 receptor over at least one of the metabotropic mGlul receptor, mGlu2 receptor and mGlu3 receptor, and preferably selective over all three thereof, are useful for the preparation of medicaments for the treatment of neuromuscular dysfunction of the lower urinary tract in mammals. A wide variety of suitable compounds is described. The medicament may contain the selective mGlu5 antagonist as the sole active agent, or may also contain one or more additional therapeutic agents for for the treatment of neuromuscular dysfunction of the lower urinary tract in mammals. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in mammals.
EP2015751A2 Salts of pyridazine compounds The invention relates to stable and substantially purified synthetic pharmaceutically acceptable acid addition salts of pyridazine compounds of the formula I wherein R10 is hydrogen, hydroxyl, alkyl, alkoxy, alkenyl, alkynyl, alkylene, aryl, heteroaryl, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, =S, carboxyl, carbonyl, carbamoyl, carboxamide, or phosphonate, and R11 is alkyl, alkoxy, alkenyl, alkynyl, alkylene, alkenylene, alkenyloxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, =S, phosphonate, carboxyl, carbonyl, carbamoyl, carboxamide, or ureido. The invention also relates to formulations, dosage forms and compositions comprising the salts, and methods of using the salts, formulations, dosage forms and compositions.
EP1743631A2 Use of an amphetamine composition for regulating memory consolidation The invention relates to the use of an amphetamine composition comprising one or more amphetamine compounds and enantiomerically enriched in an 1-amphetamine or in an 1-methamphetamine, for the manufacture of a medicament for improving memory consolidation in a human having an impairment in memory consolidation. The composition comprises at least 51 mole percent 1-amphetamine or 1-methamphetamine, relative to total amphetamine content of the composition. The invention makes available methods and reagents for enhancing and/or restoring long-term memory function and performance, e.g. to improve long-term memory (LTM) and recall ability in animal subjects.
CN1968706A Treatment with cisplatin and an EGFR-inhibitor The present invention provides a method for manufacturing a medicament for treating tumors or tumor metastases, characterized in that a therapeutically effective amount of an EGFR kinase inhibitor and cisplatin is used, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase ihibitor and cisplatin combination in combination with a pharmaceutical acceptable carrier. A Preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlotinib HC1 (also known as Tarceva).
US20050148521 Coadministration with non-steroidal antiinflammatory agent allows for lower dosage of cyclophosphamide; side effect reduction; kits The present invention relates to the surprising discovery that the combination of several agents, each well known for its established role in treating cancer, inflammation, hemostasis, bone resorption or serving as a solubilizing vehicle, results in a synergistic anti-cancer composition. Furthermore, the combination of at least three agents allows the cytotoxic agent, such as cyclophosphamide, to be used at a lower dosage than when administered alone. One predicted consequence of this treatment, therefore, is a highly desirable reduction in toxic side effects due to the cytotoxic agent.
CN101456918B Sealwort polysaccharide and preparation method thereof, and its application in preparing hypoglycemic and reducing blood lipid drugs The invention provides a polygonatum canaliculatum polysaccharide and a preparation method thereof. The polygonatum canaliculatum polysaccharide is extracted from the perennial liliaceae herbal plant of polygonatum canaliculatum and has the molecular weight of 5,000 to 100,000 Daltons. The solid polygonatum canaliculatum polysaccharide is off white or white. The monosaccharide consists of pyrane type beta-D-galactose, D-glucose and D-mannose. The product can be developed into medicines capable of reducing blood sugar and blood fat. The preparation method is reliable and feasible, and is suitable for the volume product without environmental pollution. The preparation method has low cost.
US7439269 application of moisturizer to nasal cavity may facilitate and/or promote healthy function of the cavity, which in turn may reduce the duration of symptoms associated with a common cold or the flu; comprising: purified water; a hydrophilic thickener; and an encapsulated moisturizing agent An improved composition and method for moisturizing a nasal membrane are disclosed. The composition includes a viscous carrier and one or more moisturizing agents disposed with the carrier. The composition is applied to a portion of a nasal membrane using a spray, a swab applicator, or a similar application device.
US20110190384 siRNA Specific to WT1 17AA(-)Isoform and Use Thereof Disclosed is a polynucleotide having at least 15 contiguous bases in the base sequence of SEQ ID NO:26 and including the base sequence of SEQ ID NO:27. Also disclosed is siRNA produced based on the polynucleotide. By means of this, a cancer cell-specific molecular-targeted therapy, which successfully controls the function of WT1, can be realized.
CN102716138A Medicinal composition of diammonium glycyrrhizinate sodium chloride The invention discloses a medicinal composition of diammonium glycyrrhizinate sodium chloride. The medicinal composition of the diammonium glycyrrhizinate sodium chloride is characterized in that diammonium glycyrrhizinate sodium chloride injection comprises 0.6 gram of diammonium glycyrrhizinate, 9.0 grams of sodium chloride and 1,000 milliliters of water for injection. The medicinal composition of the diammonium glycyrrhizinate sodium chloride solves the problem that the diammonium glycyrrhizinate sodium chloride injection is not provided clinically at present.
US20100240679 4-Phenylpiperidine Derivatives as Renin Inhibitors Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
CN102973417A Pharmaceutical and cosmetic compositions containing oxy group-bearing aromatic aldehydes Disclosed are pharmaceutical and cosmetic compositions containing oxy group-bearing aromatic aldehyde compounds or acetal derivatives thereof. Some of the disclosed compositions are useful as topical therapeutics for treating inflammatory dermatologic conditions. Some of the compositions are useful in transdermal and other systemic dose forms for treating other inflammatory conditions in mammals.
CA2377621C Use of nitroxides in wound healing and in the prevention of photodamage Methods for preventing photoaging and other types of sun damage and promoting wound healing by topically apply-ing a nitroxide containing compound are provided. Pharmaceutical compositions comprising nitroxide containing compounds for the prevention of photoaging and other types of sun damage and promoting wound healing are also provided.
CN1981760A Injection tyxolazo and its making method A freeze-dried powder injection of Taituolazuo is proportionally prepared from Taituolazuo, excipient and pH regulator. Its preparing process is also disclosed.
EP2754445A2 Electricity-generating particulates for use in excessive sweating The invention features a galvanic particulate, for use in a method of excessive sweating, including a first conductive material and a second conductive material, wherein both the first conductive material and the second conductive material are exposed on the surface of the particulate, wherein the particle size of the particulate is from about 10 nanometers to about 100 micrometers, wherein the second conductive material comprises from about 0.01 percent to about 10 percent, by weight, of the total weight of the particulate, and wherein the difference of the standard potentials of the first conductive material and the second conductive material is at least about 0.2 V.
CN101596159A New taxol injection and preparation method thereof The invention researches a new preparation method by aiming at the problems of large side effect, low yield, and the like of the production and the clinical application of a taxol injection and the taxol injection achieves the purposes of convenient use, cost reduction, curative effect guarantee and side effect reduction.
US20080102092 Animal extract from scallop shells; grinding, crystal structure; skin disorders An anti-Trichophyton film containing calcium hydrogen carbonate and an anti-Trichophyton forming agent enable easy formation, on a human skin, of an antibacterial film containing calcium hydrogen carbonate while assigning antibacterial effect possessed by a natural material thereto by using scallop shell as a raw material, and form an antibacterial film of calcium hydrogen carbonate with the antibacterial effect of the natural material added thereto through a simple structure, thereby enhancing the curative effect to athlete's foot. The anti-Trichophyton film forming agent is obtained by mixing a powder obtained by calcinating scallop shell mainly composed of calcium carbonate with distilled water. Remedies for dermatophytosis are prepared by grinding and calcinating scallop shells having a crystalline structure due to the calcite structure of calcium carbonate.
US7166303 An aqueous solution comprising of propofol, poloxamers; noncontamination, stability Propofol solubilised in aqueous micellar preparations of poloxamers is stable at low concentrations and that such preparations are effective administration forms for Propofol.
CN102091050A Stable simvastatin oral tablet and preparation method thereof The invention provides a stable simvastatin oral tablet which is prepared from the following components in percentage by weight: 10-20% of simvastatin, 0.01-0.04% of antioxidant, 0.5-2.0% of acidifier, 70-80% of filler, 5-10% of disintegrant, 1-1.2% of lubricant and 0.5-2% of binder. The invention also provides a method for preparing the stable simvastatin oral tablet. By strictly controlling the moisture of a finished product, the doses of the antioxidant and acidifier in the components are obviously reduced, the product stability is better, and the safety is higher.
US20100087424 Tricyclic nitrogen containing heterocycles as antibacterial agents Tricyclic nitrogen containing compounds and their use as antibacterials.
WO2013049293A1 Monoacylglycerol lipase inhibitors for the treatment of metabolic diseases and related disorders Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes. Such compounds are represented by formula (I) as follows: wherein Y and Z are defined herein.
WO2014028543A1 Arry-520 for use in treating cancer in a patient with low aag The compound ARRY-520 for use for treating cancer in patients with low [AAG] is provided.
EP2661265A1 Quinolines and aza-quinolines as crth2 receptor modulators The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J1, Ja, Jb, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with with uncontrolled or inappropriate stimulation of CRTH2 function.
US7144873 Therapy for anticancer agents, blood disorders; dissolving in nonaqueous solvent Pharmaceutical formulations, kits and vessels are provided for delivering decitabine to a patient suffering from a disease in need of treatment with decitabine. The pharmaceutical formulation comprises decitabine solvated in a non-aqueous solvent that comprises glycerin, propylene glycol, polyethylene glycol, or combinations. Such formulations are more chemically stable than conventional liquid formulations of decitabine containing more than 40% water in volume. The pharmaceutical formulations can be used for any disease that is sensitive to the treatment with decitabine, such as hematological disorders and cancer.
CN102336770A Penicillanic 1, 1-dioxide (sulbactam) composition and ester, sale and preparation method thereof The invention relates to a penicillanic 1, 1-dioxide (sulbactam) composition in line with Equation (I) in pharmacy, ester thereof, salt thereof, a composition of ester thereof, a composition of salt thereof and a preparation method of ester thereof and salt thereof. R is H, Na or KO-CH2R3; R3 is H, halogen or -OCOR33; and R33 is an alkyl group containing 1-5 carbon atom(s). The invention includes a treatment process for the compound in line with Equation (II), wherein X is manganese-containing H or Br (manganese in a powder state is mixed in an acidic medium prepared via mixing of water and organic solvents). The compound prepared in the invention can be used for manufacturing antibiotics.
EP2029544A1 Pyrrolidine derivatives useful as bace inhibitors Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class in the treatment of a disease that depends on the activity of beta- secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound. The substituted pyrrolidine compounds are especially of the formula (I), wherein the substituents are as defined in the specification.
WO2007007656A1 Pharmaceutical composition containing thiazolidinedione compound It is intended to provide a pharmaceutical composition which contains a thiazolidinedione compound and is excellent in drug absorbability. The pharmaceutical composition is a pharmaceutical composition in which cellulose, a cellulose derivative, a polyvinyl alcohol derivative, a polyvinyl alcohol derivative mixture or a mixture thereof is blended in 5-{4-[(6-methoxy-1-methyl-1H-benzimidazole-2-yl)-methoxy]benzyl}thiazolidine-2,4-dione or a pharmacologically acceptable salt thereof.
WO2013037964A1 Anticancer active ingredient derived from guiera senegalensis A compound of formula (I), a positional or structural isomer thereof, or a pharmaceutically acceptable base addition salt or acid addition salt thereof, use thereof as a medicament, in particular an anticancer medicament.
CN102716087A Vitamin powder and preparation method thereof The invention mainly discloses vitamin powder and a preparation method of the vitamin powder. The vitamin comprises the following components in mass percentage: 5-60% of fat soluble vitamin, 30-70% of wall material, 5-30% of assistant wall material, 0.5-2% of emulsifier, 0.1-2% of antioxidant and 0.1-3% of cross linking agent. The invention further relates to a preparation method of the vitamin powder. By using a microencapsulation technique, the fat soluble vitamin oil (e.g. vitamin A, vitamin D3, vitamin E and vitamin K) is embedded to a micro-capsule, the wall material used in the embeeding process is starch sodium octenylsuccinate, the vitamin oil is embeeded in the wall and then the micro-capsule is subjected to cross linkage, mist spraying and drying are carried out to form the vitamin powder, and the embedding rate of the vitamin is more than 95.3%. According to the invention, the process is simple, the cost is low, the obtained vitamin powder is not soluble in water, high in oil loading amount and good in flowability, and can be used in the fields such as foods, daily-used industrial chemicals and medicines.
US20110052664 Antimicrobial Medical Dressings and Protecting Wounds and Catheter Sites An antimicrobial medical dressing provides a combination of antimicrobial agents in various concentrations that protect against microorganisms, absorb exudates, and promote healing. The antimicrobial agents may include compositions of ethanol, hydrogen peroxide, and/or ethylenediaminetetraacetic acid.
US7285551 For use as therapeutic agent and prophylactic agent for hepatitis C The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. The compound of the present invention shows an anti-hepatitis C virus (HCV) action based on the HCV polymerase inhibitory activity, and is useful as a therapeutic agent or prophylactic agent for hepatitis C.
US6995155 Imines such as 4-(3-((3-(2,4-dichlorophenyl)propanoyl)amino)-1-(3-(morpholin-4-yl)propyl)-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-5-yl)benzamide, administered for prophylaxis of Alzheimer's disease Compounds of formula (I) are disclosed. The compounds inhibit the action of gamma secretase, and hence find use in the treatment and prevention of Alzheimer's disease.
CN1985883B Antifungal medicine composition and its preparing method and use The antifungal medicine composition is medicine prepared with the materials including snake oil 50-100 weight portions, Miconazole nitrate 25-50 weight portions, flavescent sophora root 20-50 weight portions, pearl powder 1-10 weight portions, menthol 1-5 weight portions, and borneol 1-5 weight portions. The antifungal medicine composition as one compound Chinese and Western medicine preparation contains effective antifungal components, and components for clearing away heat and toxic material, eliminating swelling, relieving pain, astringing and promoting granulation. It is used in treating tinea corporis, tinea cruris, tinea manuum, tinea pedis, etc caused by mycotic infection, and has stable treating effect and little side effect.
US8022074 4-(phenyl-piperazinyl-methyl)benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders The invention relates to at least one compound of general formula I wherein R1 is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R1 phenyl and R1 heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF3, methyl, iodo, bromo, fluoro, and chloro; R2 is independently selected from ethyl and isopropyl; R3 is hydrogen or fluoro; R4 is —NH2 or —NHSO2R5; and R5 is hydrogen, —CF3, or C1-C6 alkyl, or pharmaceutically acceptable salts thereof; at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one δ receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I.
EP0784429B1 Therapeutic combinations of venous dilators and arterial dilators A therapeutic mixture comprising a mixture of L-arginine and an agonist of nitric oxide synthase, namely nitroglycerin, is disclosed for the treatment of diseases related to vasoconstriction, wherein the vasoconstriction is relieved by stimulating the constitutive form of nitric oxide synthase (cNOS) to produce native nitric oxide (NO). The native NO having superior beneficial effect when compared to exogenous NO produced by an L-arginine independent pathway in terms of the ability to reduce clinical endpoints and mortality.
US20120277236 Method for inhibiting mmp-9 dimerization A method of inhibiting matrix metalloproteinase 9 (MMP-9) dimerization without substantially inhibiting the catalytic activity of MMP-9, comprising contacting the MMP-9 with a small molecule compound of the structure wherein A is a ring structure which is substituted by R2, R3 and R4; X is present or absent and when present is NH, O, ester or N-monosubstituted amide; Z is S, O, or N; n is an integer from 0-5; R1 is alkyl, aryl, heteroalkyl, or heteroaryl, each with or without substitution; and R2, R3, and R4 is each present or absent, and is each independently H, alkyl, aryl, heteroalkyl, heteroaryl, each with or without substitution, or a pharmaceutically acceptable salt thereof.
CN1943574A Method for preparing tinidazole dispersion tablet and use The invention discloses a preparation method and application for tinidazole dispersing tablet. Said tinidazole dispersing tablet in the invention has merits of convenient for use, fast absorption, high biological utilization ratio, etc. also featuring simple technique , stable quality, convenient for carrying and storing. The amount of tinidazole contained in each tablet of Said tinidazole dispersing tablet in the invention can be 0.2g.,0.25g.,0.5g. The main clinical use for said medicine is applying to all sorts of infection from anaerobe, colon and rectum operation, operation for gynecology and obstetrics, etc.
CN103316044A Composition structure used for inhibiting gastrointestinal bacterial infections The invention provides a composition structure used for inhibiting gastrointestinal bacterial infections. The structure comprises a main layer and active particles. The main layer is prepared by using a carbon material, and the active particles are loaded on a surface of the main layer. The active particles are prepared from a material of a group of components selected from silver, gold, aluminum, zinc, copper and titanium dioxide.
CN1615849A Armillarisin A for injection and its preparing method The armillarisin A for injection has raised armillarisin A stability and raised armillarisin A quality. The soft armillarisin A for injection contains armillarisin A as active component in 5-45 mg, preferably 10-40 mg, excipient and co-solvent 5-10 %, pH regulator in 0.1-2 %, and antioxidant stabilizer in 0.01-0.6 % for raised antioxidant performance.
EP1838294A1 Compositions comprising pde4 modulators and their use for the treatment or prevention of airway inflammation Methods of treating, preventing, and managing airway inflammation and other airway or pulmonary diseases and disorders are disclosed. Specific methods comprise the administration of a PDE4 modulator, or a pharmaceutically acceptable salt, solvate, stereoisomer, or prodrug thereof, alone or in combination with a second active agent and/or other conventional therapies. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
CN101926771A Acylated amylopectin-modified BCG-polysaccharide nucleic acid oral veterinary liposome and freeze-dried preparation thereof The invention belongs to the field of animal medicaments, and discloses an acylated amylopectin-modified BCG-polysaccharide nucleic acid oral veterinary liposome and a freeze-dried preparation thereof. The liposome formula contains the following raw materials in part by weight: 1 part of BCG-polysaccharide nucleic acid, 1 to 10 parts of acylated amylopectin, 10 to 50 parts of phospholipid and 1 to 10 parts of cholesterol. The liposome and the freeze-dried preparation have the advantages of good safety, remarkable improvement of stability, good encapsulation effect and improvement of compliance and safety for animal use.
WO2005030779A3 Laulimalide analogs with anti-cancer activitity The present invention provides compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein R1-R10, q, t, X0, X1, A, B, D, E, G, J, K, L, M and Z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders associated with cellular hyperproliferation.
WO2014034756A1 Pharmaceutical composition for use in treatment of status epilepticus The present invention relates to the provision of a pharmaceutical composition for use in the treatment of status epilepticus or a method for treating status epilepticus. The present invention provides a pharmaceutical composition for use in the treatment of status epilepticus, which comprises a GABA agonist and perampanel or a pharmacologically acceptable salt or hydrate thereof.
US7074782 Administering to a patient suffering from caspase mediated diseses, an effective amount of a mono,bi or tri-heterocyclic ring containing nitrogen atom attached to ester or thioester to form carbamate group, as caspase inhibitor This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
EP1666037A2 Compositions for stimulating neurite growth The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.
CA2176719C Fatty acid delivery system Delivery to the colon of fatty acids especially Short Chain Fatty Acids (SCFA) can be effected by covalently linking SCFA to a carrier that is preferably a form of carbohydrate, by an ester link. The SCFA is protected by its link with the carbohydrate through the small intestine, and where the carbohydrate is digestible in the small intestine such as a digestive starch, the starch can also be protected from digestion in the small intestine by the substitution. Levels of SCFA such as acetate, propionate and butyrate may be elevated to have beneficial effects in the prevention of colonic disorders such as rectal cancer, diverticulitis, colitis, diarrhea and constipation.
CN103006582A Salvianolic acid A lyophilized powder injection and application thereof in preparation of drugs The invention relates to a salvianolic acid A lyophilized powder injection, which comprises 10-80g of salvianolic acid A, 10-80g of filling agent, and an antioxidant accounting for 0.01%-0.2% of the total amount of the preparation. The freeze drying process of the preparation method comprises the following steps: A. freezing: reducing the temperature to -40 DEG C to -45 DEG C at the speed of 20 DEG C to 30 DEG C per hour, and freezing for 10-16 hours under thermal-insulation condition; B. sublimating: vacuumizing to below 0.3 mbar, raising the temperature of the frozen salvianolic acid A preparation to -23 DEG C to -27 DEG C in 10-14 hours, and vacuum drying for 6-8 hours while maintaining the temperature at -23 DEG C to -27 DEG C; and C. drying: heating up, uniformly raising the temperature to 40 DEG C to 45 DEG C at the speed of 0.5 DEG C to 1.0 DEG C per minute, drying for 2-5 hours while maintaining the temperature at 40 DEG C to 45 DEG C, then reducing the sample temperature to the room temperature, and capping to obtain the salvianolic acid A lyophilized powder injection. The invention also discloses the application of the salvianolic acid A lyophilized powder injection in preparation of drugs.
US20080275009 Oral administration of n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-1,3-thiazole-5-carboxamide and salts thereof Disclosed are a method of treating cancer and/or other proliferative diseases comprising orally administering N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide or a salt thereof, and pharmaceutical compositions comprising N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide or a salt thereof. Also disclosed are N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide salts, as well as crystalline forms thereof.
CN102875617A Geniposide derivative, preparation method thereof and application of geniposide derivative to inflammation resistance The invention discloses a geniposide derivative. In the general structural formula, R1 is -OR'1, -S R'2, or -NR'2 R'3, R'1 is H or alkyl with 1 to 6 carbon atoms, R'2R'3 is H, fat alkyl with 1 to 6 carbon atoms or aromatic alkyl; R2 is -O R'4; and R'4 is H, CH4 or acyl. The invention also discloses a preparation method for the geniposide derivative. The preparation method briefly comprises the following steps of: acylating geniposide to obtain a derivative; hydrolyzing and acylating geniposide to obtain a derivative; reacting to obtain a derivative under the action of a condensing agent; and generating a derivative in a methanol solution of ammonia. The invention also discloses application of the geniposide derivative to inflammation resistance, and the application is explained through verification tests. The preparation method has the advantages that the novel derivative is prepared by performing derivatization reaction on the geniposide; the preparation method is successfully applied to the technical field of inflammation resistance on the basis of the derivative; and a good effect is achieved.
WO2012016367A1 Trehalose derivatives, preparation methods and uses thereof Trehalose derivatives shown as the general formula (I), preparation methods and uses thereof in the manufacture of medicines for preventing and treating invasion and metastasis of colon cancer 26-L5 cells are disclosed, wherein R is defined as in the description.
CN102977082A Isocoumarin compound as well as preparation method and application thereof The invention provides an isocoumarin compound, a preparation method thereof and application of the isocoumarin compound in preparing antibiotic medicaments and antineoplastic medicaments. The lateral chain of the isocoumarin compound is in a unique hexahydro-pyrimidine ring structure; and the isocoumarin compound provided by the invention is obtained by fermenting and separating bacillus subtilis strains, has broad-spectrum bacteriostasis activity and higher antibacterial activity on both gram-positive bacteria and gram-negative bacteria and shows higher tumor resistance.
WO2012064808A1 Tetrazolyl - tetrahydropyridine compounds for inflammation and immune - related uses The invention relates to certain compounds according to formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
WO2006013873A1 Drugs having cyclooxygenase inhibiting activity Drugs having cyclooxygenase inhibiting activity, preferably cyclooxygenase 2 selective inhibiting activity, which contain as the active ingredient compounds represented by the general formula (I) or salts thereof: (I) wherein X is an optionally substituted connecting group whose main chain is composed of 2 to 5 atoms; A is hydrogen or acetyl; E is optionally substituted aryl or optionally substituted heteroaryl; and Z is arene which may have a substituent in addition to the groups represented by the general formulae: -O-A and -X-E or heteroarene which may have a substituent in addition to the groups represented by the general formulae: -O-A and -X-E.
CN102068422B Medical use of (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid The invention discloses a medical use of (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid. Further, the (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid can be used for preparing analgesic and anti-inflammatory or anti-tumor medicaments containing the (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid or pharmaceutical acceptable salts thereof.
US20100291240 Method to Stabilize a Dietary Supplement to Facilitate Joint Health in Humans The present invention provides for compositions comprising glucosamine wherein the glucosamine has improved and/or enhanced stability. Additionally, the present invention provides for methods of stabilizing compositions for use in preparing an oral dosage form comprising glucosamine.
WO2008037415A1 Use of theanine for producing a drug for use in the prophylaxis and treatment of psychiatric disorders of the central nervous system, especially of depressions and pains Theanine, its derivative or its pharmaceutically acceptable salts can be used for producing a drug for use in the prophylaxis or treatment of psychiatric disorders of the central nervous system, especially of depressions and pain conditions.
CN1895251A Stabilized nalmefene hydrochloride injection and its preparation A high-stability nalmefene hydrochloride injection is prepared from nalmefene hydrochloride (0.005-0.2 W/v %) and the medicinal carrier chosen from sodium chloride, glucose, beta-cyclodextrin, dextran, pectose, sorbitol, etc. Its preparing process is also disclosed.
US20080069831 Vaccines; fusion protein; induce immunology response Disclosed are compositions, including vaccines, and methods for vaccinating an animal against hepatitis C virus (HCV) and for treating or preventing hepatitis C viral infection in an animal. The invention includes a variety of novel HCV fusion proteins that can be used directly as a vaccine or in conjunction with a yeast-based vaccine vehicle to elicit an immune response against HCV in an animal. The invention also includes the use of the HCV fusion gene and protein described herein in any diagnostic or therapeutic protocol for the detection and/or treatment or prevention of HCV infection.
CA2553423C Heterocyclic compounds for use in the treatment of cancer and the inhibition of angiogenesis Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutically compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
US7629347 Modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases; cancer; chronic myelogic leukemia The present invention relates to uses of the compounds of Formula I as well as pharmaceutically acceptable salts and stereoisomers thereof in methods to treat a variety of tumors in mammals involving abnormal tyrosine kinase signaling, the compounds represented as: wherein R1 and R2 are independently selected from the group consisting of H; alkyl; alkenyl; alkynyl; halogen; aryl; heteroaryl containing N, O, or S; the aryl and heteroaryl may be further substituted with halogen, an alkyl, alkenyl, and alkynyl; NZ1Z2, wherein Z1 and Z2 are independently selected from the group consisting of H and alkyl; and (CO)Y wherein Y is selected from the group consisting of H, alkyl, alkenyl, alkynyl, aryl, heteroaryl containing N, O, or S, and the aryl and heteroaryl may be further substituted with halogen, alkyl, alkenyl, and alkynyl; with the proviso that when R1 is hydrogen, R2 is a group other than hydrogen.
US20090010869 Compositions for Topical Enzymatic Debridement Formulations are described for the treatment by enzymatic debridement of wounds and ulcers. The formulations have a clear, transparent composition that allows for easy visualization of the wound, and are non-staining for easy clean up. These formulations can also exhibit increased enzymatic debridement activity, improved post-treatment lubricity and coating occlusivity, and stability. The formulations, optionally containing non-animal source biologics, may be in the form of lotions, aerosols to provide a spray, or a foam. A non-reactive substrate may be used as a composition carrier. A non-aqueous lotion formulation having improved enzymatic activity is provided. The non-aqueous lotion viscosity is adjusted to achieve high enzymatic activity while maintaining the application benefits of high viscosity non-aqueous lotions. The lotion formulation may be delivered in a patch.
WO2008061466A1 Synthetic methods of aclatonium napadisilate and analogs thereof Disclosed are synthetic methods of formula (V) compounds: wherein R1-R7 are same or different and respectively selected from hydrogen and C1-4 alkyl; and n is an integer of 1-4. Said methods can be carried out as one-pot processes. Synthetic methods of cholinergic aclatonium napadisilate and analogs thereof are also provided.
US20110136892 Targeting TGF-beta as a Therapy for Alzheimer's Disease The invention includes compositions and methods for enhancing peripheral macrophage Aβ phagocytosis activity. The invention includes inhibiting a component of TGF-β signaling pathway in peripheral macrophages to promote central nervous system infiltration and beneficial cerebral Aβ clearance. Inhibition of TGF-β signaling in peripheral macrophages represents an advantageous anti-amyloid therapeutic approach for Alzheimer's disease.
US20100158993 Topical Gel Compositions Topical alcoholic gel compositions are disclosed that are useful for delivering therapeutic levels of an NSAID to target in and below the skin. The compositions comprise a topically active drug, an alcoholic solvent, a polymeric thickener, and optionally a keratolytic agent. In one embodiment, excellent viscosity for dermal application is attained without the need of a step for neutralizing the pH of the composition. Alcoholic and alcohol-free topical compositions comprising an NSAID prodrug are also disclosed. The compositions are particularly useful for the treatment of pseudofolliculitis barbae.
US6841553 Contorlling fertility The invention relates to a bicyclic heteroaromatic derivative compound according to general formula (II), or a pharmaceutically acceptable salt thereof. The compounds of the invention have LH receptor activating activity and can be used in fertility regulating therapies.
CN102973519A Amoxicillin granules and preparation technology of same The invention discloses amoxicillin granules and a preparation technology of the same. The amoxicillin granules are prepared by taking a pure water solution of povidone as a binding agent solution for granulation, wherein the dosage ratio of the povidone to the amoxicillin is (1:25)-(1:10) by weight percent. With the preparation technology, the production safety is improved, and the solubility and the stability of the amoxicillin granules are improved greatly.
CN101269029A Omeprazole sustained-release dropping pill and preparation method thereof The invention relates to a sustained-release omeprazole dropping pill prepared by adopting omeprazole as the ingredient. The sustained-release omeprazole dropping pill aims to supplement the deficiency of the prior oral formulation of the sustained-release omeprazole dropping pill used for gastric ulcer, duodenal ulcer, stress ulcer, reflux esophagitis and gastrinoma and provide a sustained-release omeprazole dropping pill with a longer acting time. The sustained-release omeprazole dropping pill is prepared by adopting omeprazole as the ingredient, mixing omeprazole with a hydrophilic framework ingredient, carmowax (10,000-20,000) and hydrophobic framework ingredients, stearic acid and glycerin monostearate, and coating the prepared sustained-release dropping pill with an enteric coat.
US20120028956 Bicyclic mglur5 positive allosteric modulators and methods of making and using same In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
US20080193521 Hyperphosphatemia in chronic kidney disease or end-stage renal disease patients; nutritional supplements The present invention provides compositions and methods for removing phosphate from a subject using chitosan. The present invention also provides compositions and methods for treating hyperphosphatemia based on phosphate-binding chitosan.
WO2007112322A2 Indole compounds having sphingosine-1-phosphate (s1p) receptor agonist and/or antagonist biological activity The present invention provides novel compounds having the following general formula (I) wherein: A, B, X, Y, R1, R2, R3, R4, n, o and p are as defined in the specification. Such compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions or diseases and wound healing.
WO2012158795A1 Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, Jak3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.
US7112597 5-(Substituted thiazolylethoxy)indaneacetic acid derivatives, used in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.
WO2008049832A1 Furanone derivatives as cysteine protease inhibitors Compounds of the Formula (Il) wherein R1 is H, OH, F R2 is -CH2CH(CH3)2, -CH2C(CH3)3 or -CH(CH3)(CH2CH3); R2' is H; or R2 and R2' together with the adjacent C atom defines cyclohexyl; and pharmaceutically acceptable salts, hydrates and N-oxides thereof have utility in the treatment of disorders characterised by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
US20120157378 Methods and Compositions for Predicting a Subject's Susceptibility To and Risk of Developing Type 2 Diabetes Aspects of the invention include methods of predicting a subject's susceptibility to developing type 2 diabetes. Embodiments of the methods include obtaining a sex hormone-binding globulin (SHBG) level value for the subject, e.g., by detecting a SHBG plasma concentration and/or a SHBG polymorphism phenotype, and predicting the subject's susceptibility to developing type 2 diabetes from the obtained SHBG level value. Also provided are devices and kits that find use in practicing embodiments of the methods. In addition, methods of treating a subject for type 2 diabetes and/or preventing the onset of type 2 diabetes are provided.
CN102080084A Human miR-125a-5p antisense nucleotide and application thereof The invention discloses a human miR-125a-5p antisense oligonucleotide and application thereof. The antisense oligonucleotide binds specifically to human miR-125a-5p, including a sequence which is complement to at least 13 continuous nucleotides of nucleotide sequence 5'-UCCCUGAGACCCUUUAACCUGUGA-3', specially the sequence 5'-UCACAGGUUAAAGGGUCUCAGGGA-3'. The antisense oligonucleotide in the invention can be a ribonucleoside, a deoxyribonucleotide or a chimera of the ribonucleoside and the deoxyribonucleotide. In addition, any nucleotide in the antisense oligonucleotide chain can be modified. The antisense oligonucleotide miR-125a-5p in the invention can effectively inhibit the expression of miR-125a-5p in human glioma cells, inhibit the growth and propagation of the glioma cells, and thus effectively treat glioma and other tumors with high expression rate of miR-125a-5p.
WO2013067579A1 Adiposity-modulating molecules and uses therefor Disclosed are methods and compositions for modulating adiposity-related conditions, which utilize inhibitors of phospholipase A2, and more particularly phospholipase A2 Group IIa (PLA2G2A). Representative adiposity-related conditions include obesity, type II diabetes, adipose inflammation, metabolic dysfunction, cardiovascular diseases and more generally, metabolic syndrome.
CN102552243A Application of myricanol and/or myricanone in preparing antitumor drugs The invention discloses the application of myricanol and/or myricanone in preparing antitumor drugs. The antitumor drugs include drugs for preventing and/or treating liver cancers, drugs for preventing and/or treating lung cancers, drugs for preventing and/or treating leukaemia, drugs for preventing and/or treating stomach cancers or drugs for preventing and/or treating other tumors. The study proves that myricanol and myricanone have good antitumor effects and cause low toxicity to normal cells. Myricanol and myricanone are applied to prepare antitumor drugs and have high efficacy and low toxicity. The invention conforms to the requirements for drug development.
WO2013146386A1 Sustained-release local anesthetic preparation The purpose of the present invention is to provide a sustained-release local anesthetic preparation which is a composition containing a liposome having a local anesthetic carried therein and has excellent sustainability. The sustained-release local anesthetic preparation according to the present invention comprises: a first liposome which has an outer membrane composed of a multi-layered lipid bilayer membrane; multiple second liposomes which are accommodated in a first liposome inside region defined by the outer membrane and each of which has an outer membrane composed of a multi-layered lipid bilayer membrane; and second liposome inside regions each of which is defined by the outer membrane of each of the second liposomes. In the sustained-release local anesthetic preparation, an ion gradient is formed at least between each of the second liposome inside regions and the outside of the first liposome, and a local anesthetic is contained in at least each of the second liposome inside regions.
CA2381801C Phosphonic acid derivative having inhibitory activity against carboxypeptidase b A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: (see formula I) wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents -CH2-, -O-, or -NH-; A represents the following group (II): (see formula II) [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.
US7700570 Oligonucleotide mediated specific cytokine induction and prophylaxis and treatment of viral infection in a mammal The invention provides new methods for modulating specific CMI-inducing cytokines in vivo. Such new methods result in stimulation of the cytokines IL-6, IL-12 MIP-1β and MCP without substantially inducing undesired cytokines. The methods according to the invention are based upon administration of oligonucleotides containing particular structural motifs which lead to specific cytokine induction.
CN101940569A Medicament composition containing sorafenib, artemisinin and artemisinin derivative and application thereof in preparing medicament for treating cancer The invention relates to a medicament composition containing sorafenib, artemisinin and an artemisinin derivative and application thereof in preparing a medicament for treating lung cancer, pancreas cancer, colon cancer, liver cancer, prostatic cancer, kidney cancer, stomach cancer, brain tumor, sarcoma, ovarian cancer or breast cancer. The medicament composition has remarkable synergistic effect, improves the curative effect of the medicament, reduces the administration dosage and reduces side effects.
US8362241 Inhibitors of PI3 kinase and/or mTOR The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
EP1731154A1 Immediate-release and high-drug-load pharmaceutical formulations of micronised (4-chlorophenyl)|4-(4-pyridylmethyl)pht halazin-1-yl| and salts thereof The invention relates to immediate-release and high-drug-load solid pharmaceutical formulations comprising micronised (4-chlorophenyl)[4-(4-pyridylmethyl)-phthalazin-1-yl] as well as pharmaceutically acceptable salts thereof.
US20090253700 N-'4-4(4-morpholinyl) phenyl!- '(4-piperidinyl) methyl! carboxamide derivatives and their use as glycine transporter inhibitors The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, n and Ar are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
CN102462669A Troxipide dispersible tablet and preparation method thereof The invention discloses a troxipide dispersible tablet and a preparation method thereof. The troxipide dispersible tablet contains 30-40% by weight of troxipide and 10-30% by weight of sodium carboxymethyl starch and/or cross-linked polyvinyl pyrrolidone serving as a disintegrating agent, and can further contain an adhesive, a filling agent, a sweetening agent, a lubricant and other pharmaceutical auxiliary materials. The dispersible tablet has the characteristics of short disintegration time, good dispersion uniformity, rapidness in medicament dissolution, rapidness in absorption, high bioavailability and convenience for administration.
US7056909 5,5-Difluoro-3(S)-(pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-(1, 8)-naphthyridin-2-yl)-nonanoic acid; inhibition of bone resorption, restenosis, angiogenesis, retinopathy, macular degeneration, arthritis, metastatic tumor growth, etc. The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αvβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
WO2009108067A2 Prevention and treatment of hsmi The present invention relates to the use of a compound for the preparation of a nutritional and/or pharmaceutical composition for reducing the mortality related to heart and skeletal muscle inflammation (HSMI) of a fish.
CN103554008A 1,3-substituted-5-acetaminoindolone compounds and application thereof to anti-tumor drugs The invention relates to 1,3-substituted-5-acetaminoindolone compounds and an application thereof to anti-tumor drugs. The compounds are 1-methyl-5-acetamino-2-indolinone, 1-(4-bromobenzyl)-5-acetamino-2-indolinone, 1-(4-methylbenzyl)-3-oxime-5-acetaminoindolone, 1-(4-methoxybenzyl)-3-oxime-5-acetaminoindolone and the like. The in-vitro tumor cell inhibitory activities of the 1,3-substituted-5-acetaminoindolone compounds synthesized in the invention are tested and the results show that such kind of compounds have certain inhibiting effects (IC50(100mu M)) on human leukemia cells (K562), human colon cancer cells (HT-29) and human liver cancer cells (HepG2), have anti-tumor activities and can be used for preparing anti-tumor drugs.
WO2007088277A1 Tricyclic ν-heteroaryl-carboxamide derivatives containing a benzimidazole unit, method for preparing same and their therapeutic use The invention concerns tricyclic Ν-heteroaryl-carboxamide derivatives containing a benzimidazole unit, of general formula (I) wherein: A represents, with the C-N bond of the benzimidazole unit to which it is bound, a 4- to 7-membered monocyclic heterocycle or a monocyclic heteroaryl containing from one to three heteroatoms selected among O, S or N, including the nitrogen atom of the benzimidazole unit; P represents a 8-, 9-, 10-, 11-membered bicyclic heterocycle or a bicyclic heteroaryl, comprising 1 to 6 heteroatoms selected among N, O or S; R1 represents on to four atoms or groups, identical or different; Y represents an oxygen or sulfur atom; R2 represents a hydrogen atom, a halogen atom, a C1C6-alkyl, C3-C7- cycloalkyl, C3-C7-cycloalkyl-C1-C3-alkylene, C1C6-fluoroalkyl or C1C6-alkoxy group; R3 represents from one to three atoms or groups, identical or different; in base or acid addition salt state as well as in hydrate or solvate form. The invention also concerns a method for preparing the compounds and their therapeutic use.
US20050113451 7-acetamidinyl derivatives The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
CN1785176A Soft capsule of mycophenolic acid or like and its prepn. method A softgel of mycophenolic acid or its analog is prepared from mycophenolic acid or its analog (10-90%), plant oil (salard oil) or polyethandiol (PEG 400) (20-90%, surfactant (0.8-20%), water (0.1-2%) and suspending aid (0.2-20%). Its preparing process is also disclosed.
WO2014059901A1 2'-cyano substituted nucleoside derivatives and methods of use thereof for treatment of viral diseases Compounds of Formula (I) are disclosed, wherein R1, R2, R3, R4, R5, and R18 are defined herein. The compounds encompassed by Formula (I) include compounds which are HCV NS5B inhibitors and other compounds which can be metabolized in vivo to HCV NS5B inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
WO2006103545A1 4-piperazinylthieno [2,3-d] pyrimidine compounds as platelet aggregation inhibitors Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) wherein A1 , A2, A3, A4, A5, A6, A7, A8, X4, X6, R2k, R2I, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
WO2013018779A1 CRYSTAL OF α-GLUCOSYL HESPERIDIN AND USE THEREOF The purpose of the present invention is to provide: a novel crystal of α-glucosyl hesperidin, of which the crystal structure is elucidated; a powder substantially comprising the crystal; and use of the powder as a material for a medicinal agent. The purpose can be achieved by providing: a crystal of α-glucosyl hesperidin, which has a crystallographic space group of P21, and of which the unit lattice has a lattice constant a of 13.983 Å, a lattice constant b of 7.620 Å and a lattice constant c of 20.065 Å, and which is a monoclinic crystal wherein α = γ = 90˚ and β = 93.475˚; a powder substantially comprising the crystal; and use of the powder as a material for a medicinal agent.
EP2221047A1 Reverse-micellar delivery system for controlled transportation and enhanced absorption of agents The invention can be summarized as follows. The present invention provides a reverse-micellar delivery system for enhanced absorption of an agent of interest across biological membranes such as the gastro-intestinal tract of mammals. The reverse-micelles comprise at least one ionic amphipathic compound, and at least one polar active agent ionizable in aqueous or physiological media. The delivery system facilitates transportation of the agent across the gastro-intestinal tract or other membranes and enhances the in-vivo release and availability of the agent(s) of interest within a fluid environment.
CN101239990B N-(2,3,4,5,6-pentahydroxyhexyl)-L-amino acid platinum ligand, preparation method and application thereof The invention discloses a kind of platinum anti-tumor compound with low nephrotoxic, and preparation and application in anti-tumor treatment thereof are also discloses. The inventive compound has definite anti-tumor activity according to in vitro and in vivo tests. In comparison with cisplatin, the inventive compound can reach the same distribution in tumor tissue when used in treatment of tumor,but the distribution in vitals such as kidney is much lower, and a much higher content level of platinum in urine and manure is kept, so as to discharge platinum by urine. Thus nephrotoxic is not showed, and the compound can be used in treatment of tumor safely and effectively.
CN101822659A Application of colchicin in preparing cholestatic liver disease drug The invention relates to application of colchicin in preparing drugs, in particular to application of colchicin in pharmacotherapy of cholestatic liver disease, the application of colchicin in preparing a cholestatic liver disease drug, and the application of colchicin in preparing the drug for treating gestation intrahepatic cholestasis syndrome, inner primary cirrhose biliaire, primary sclerosing cholangitis severe jaundice or immunity jaundice cholestatic liver disease. The colchicin can effectively lower liver injury and cholestasis caused by cholestatic liver disease, i.e. the colchicin can effectively treat cholestatic liver disease. The colchicin can effectively lighten hepatic cell necrosis, inflammatory cell infiltration and bile capillary hyperplasia caused by cholestasis. The colchicin can effectively increase bile acid, bilirubin and expression of phospholipid transporters BSEP, MRP2 and MDR3 in a bile duct, accelerates excretion of bile acid, bilirubin and phospholipid deposited in the body and reduces liver damage.
EP1549301A2 A method for using tethered bis(polyhydroxyphenyls) and o-alkyl derivatives thereof in treating inflammatory conditions of the central nervous system The present invention involves the use tethered bis(polyhydroxyphenyl) compounds to slow the progression of neurological diseases in which pro-inflammatory cytokine stimulation of microglial cells is reasonably anticipated to make a significant contribution to disease pathology. Diseases for which this is the case include amyotrophic lateral sclerosis (AlS) and other motor neuron diseases (MNDs) of similar clinical presentation; Parkinson's disease (PD); Alzheimer's disease (AD); spino-bulbar atrophy; (SBA); Huntington's disease (HD); myasthenia gravis (MG); multiple sclerosis (MS); HIV-associated dementia; fronto-temporal dementia (FTD); stroke; encephalomyelitis; traumatic brain injury; age-related retinal degeneration; and other neurological diseases possessing microglial activation as a contributing pathological feature. Specific examples are presented where the tethered bis(polyhydroxyphenyl) compound is resveratrol; piceatannol; nordihydroguaiaretic acid (NDGA), curcumin, or sesamin.
CN101766813A Suppository for treating mammalian endometritis and preparation method thereof The invention discloses a suppository for treating mammalian endometritis and a preparation method thereof; the suppository comprises the following ingredients by counting total weight of the preparation: 0.001-0.1 percent of lysostaphin, 0.1-10 percent of lysozyme, 0.1-10 percent of sodium alginate tech grade, and 80.0-99.6 percent of polyoxyethylene ascorbyl stearate; by adopting the local administration mode, the mammalian endometritis can be effectively treated, the sterilizing effect is strong, the stability is good; in addition, in the processing process, as the lysozyme and the lysostaphin are packaged by the sodium alginate tech grade, so as to keep the activity of the enzymes in the suppository preparation process, lead the enzymes to be released in utero slowly and achieve better curative effect.
EP1392241B1 System for osmotic delivery of pharmaceutically active agents An osmotic system for delivering a pharmaceutically active agent which comprises a core portion, a layer portion enclosing the core portion, and a semipermeable wall portion enclosing the core portion and the layer portion. The core portion includes the pharmaceutically active agent at a first concentration. The pharmaceutically active agent is present in the layer portion at a second concentration. The second concentration is greater than the first concentration. Such a system provides for the osmotic release of the pharmaceutically active agent in release profile other than a zero order release profile, and wherein the release profile is similar to or approaches or reaches a first order release profile.
EP2662082A1 Administration of mTOR inhibitors Disclosed are methods for treating a patient with an mTOR inhibitor such as AP23573, sirolimus, temsirolimus, everolimus, etc.
CA2353048C Pharmaceutical composition useful in the prevention or treatment of peptic ulcers An inhibitor composition of Helicobacter pylori adhesion in the stomach comprises (1) anti-urease antibodies obtained from eggs laid by hens which have been immunized against H. pylori urease and (2) an inhibitor of gastric acid secretion. This inhibitor is capable of completely eliminating H. pylori from the stomach, so it is useful for the prevention or treatment of diseases caused by infection of H. pylori such as peptic ulcers.
US20060039962 Amphiphilic compounds and vesicles liposomes for organ-specified drug targeting An amphiphilic compound is provided capable of forming vesicles or liposomes, said amphiphilic compound having at least one headgroup containing a selectively cleavable group or moiety such as a residue of a choline or phenylalanine derivative, and at least one hydrogen-bonding group located either within said headgroup and/or in close proximity thereto. The cleavable group or moiety is cleaved under selective conditions including change of chemical, physical or biological environment and is preferably cleaved enzymatically in a biological environment such as the brain or the blood. Vesicles or liposomes made from said amphiphilic compounds are suitable for delivery of a therapeutic substance or a diagnostic agent specifically to a target organ or tissue, or for delivery of a nucleic acid for gene therapy.
US20110150889 Haemophilus influenzae type iv pili The invention described herein relates to a Haemophilus influenzae (H. influenzae) regulon encoding type IV pili. In particular, the invention relates to type pili from nontypeable H. influenzae (NTHi) and from H. influenzae strains a, b, c, e and f. The invention provides isolated H. influenzae pilus polynucleotides and polypeptides encoded by the polynucleotides as well as polynucleotides and polypeptides encoded by the polynucleotides involved in the assembly/disassembly of the structure. The invention also relates to uses of these polynucleotides and/or polypeptides including methods for eliciting an immune response to H. influenzae and methods of treating and preventing H. influenzae related pathological conditions.
EP2751076A1 Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; -CH2-O-C(=O)Me; R8 is OProt°, where Prot° is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) -C(=O)-ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) -CH2-O-C(=0)RC2, where RC2 is methyl or phenyl; (iii) -CH2-O-Si-(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) -C(-YRC3)(-YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.
WO2007002173A1 Hiv-1 protease inhibitors, and methods of making and using them One aspect of the invention relates to the design, synthesis and biological activity of novel HIV-1 protease inhibitors incorporating N-phenyloxazolidine-5-carboxamides into the (hydroxyethylamino)sulfonamide scaffold as P2 ligands. For example, the present invention relates to inhibitors with variations at the P2 phenyloxazolidine and the P2' phenylsulfonamide moieties. Remarkably, compounds with an (S)-enantiomer of substituted phenyloxazolidines at P2 show highly potent inhibitory activities against wild-type HIV-1 protease. In certain embodiments, the inhibitors of the invention have Ki values in low picomolar (pM) range. In certain embodiments, the inhibitors of the invention were shown to be active against a variety of multi-drug resistant (MDR) HIV-1 proteases, each representing different paradigm of drug resistance.
WO2009051660A2 Compounds for activating tgf-beta signaling Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-β signaling are described.
CN102139020A Medicament for treating influenza and bad cold and preparation method thereof The invention discloses a medicament for treating influenza and bad cold and a preparation method thereof. The medicament is prepared from green tea and crystal sugar according to a certain weight ratio. The medicament has the effect of stimulating high-level nervous centralis to excite spirit, can expand coronary blood vessels and peripheral blood vessels and loosen smooth muscles, is used for treating the influenza and the bad cold, and has quick curative effect and high cure rate.
CN101967138A Fatty acid schisantherin A ester compound The invention discloses a fatty acid schisantherin A ester compound. The compound has the following general formula which is shown in the specification, wherein R= is an n-propyl group, an n-butyl group, an n-pentyl group, an n-hexyl group, an n-heptyl group or an n-nonyl group. Researches show that the compound is an inhibitor of differentiation protein Id1 and is prepared from schisantherol A serving as a raw material by acylation reaction; and the compound can be used as the inhibitor of differentiation protein Id1, a human glioma cell line resistance U87 medicament or the inhibitor of nuclear factor kB (NF-kB).
CN102961478A Anti-inflammatory and anti-allergic composition and preparation method for same The invention discloses an anti-inflammatory and anti-allergic composition and a preparation method for the same. The composition is mainly composed of 30-90 parts by weight of kirilow groundsel herb, 10-30 parts by weight of fingered citron, and 0.1-1 parts by weight of cysteine. The main ingredient of the composition disclosed by the invention is kirilow groundsel herb, and supplemented by fingered citron and cysteine; the ingredients are mutually harmonized, promoted and enhanced, so as to generate a good synergistic effect; and experimental verification indicates that the composition has a good anti-inflammatory and anti-allergic function. Moreover, the composition is definite in constituents, moderate in efficacy, safe and reasonable, simple and practicable in process, and good in application prospect and market prospect.
CN101104618B Long chain alkyl berberine salt derivative, synthetic method and use The present invention relates to a class of chemically named long chain alkyl berberine salt derivatives (hydrochloride or Bromate or iodate or hydrofluoric acid salt), and the molecular structural formula is stated above, wherein, X is equal to F-, Cl-, Br-, I-, SO42-, NO3-, PO43-, citric acid radical, acetic acid radical or lactic acid radical. R1, R2, R3, R4, R5 see table above. The class of the substances is provided with obvious hypoglycemic and hypolipidemic activities which are significantly higher than that of berberine salt, so that the invention is a very promising new compound withhypoglycemic and hypolipidemic medicinal values.
US20100256193 Pharmaceutical formulations comprising nitrocatechol derivatives and methods of making thereof The present disclosure relates to compositions and pharmaceutical formulations comprising at least one active pharmaceutical ingredient chosen from nitrocatechol derivatives of formula I as defined herein and salts, esters, hydrates, solvates and derivatives thereof and methods of making said compositions and pharmaceutical formulations.
CN1754539A Tetrodotoxin oil phase formulation preparation method The invention also relates to the process for preparing oil phase preparation of Tetrodotoxin, which comprises dissolving Tetrodotoxin into solution of acidic water or acidic alcohols, then mixing with one or more surface active agent, medical oil and anti-oxidant. The oil preparation can be made into the forms of capsules, emulsion, nourishing agent or suppository.
WO2014129989A1 3-substituted-6h-benzo[c]chromen-6-ones and 3-substituted-7,8,9,10-tetrahydro-6h-benzo[c]chromen-6-ones against senile dementia This invention is related with the conversion of xenobiotics to potent ACHE and BCHE inhibitors that have activity comparable to the current ACHE and BCHE inhibitor drugs (i.e., donepezil, rivastigmine, and galantamine).
EP1996561A1 Bicyclic heterocycles, medicaments containing these compounds, their use and process for preparing them The present invention relates to bicyclic heterocycles of the general formula (I), their tautomers, their stereoisomers, their mixtures and their salts, in particular physiologically tolerable salts with inorganic or organic acids, which have valuable pharmacological properties, in particular an inhibiting action on the signal transduction transmitted by tyrosinekinases, their use for the treatment of illnesses, in particular tumours and also benign prostatic hyperplasia (BPH), of disorders of the lungs and the bronchia and their preparation.
CN1965832A Compound injection of idazoxani hydrochloride and preparation process thereof The invention provides a compound benzoxyazole hydrochloride injection, wherein the preparing process consists of dissolving benzoxyazole and dipunorfen hydrochloride into distilled water, merging into miscible liquid solution wherein ml contains benzoxyazole hydrochloride 10-25mg, dipunorfen hydrochloride 0.1-0.3mg, sealing and sterilizing. The injection is used for waking animals quickly after anaesthetizing.
US8623877 Substituted N-heteroaryl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.
CN1875990A Pharmaceutical composition with anticancer activity The invention relates to a medicinal combination of cantharidin, secretio bufonis, ginseng saponin, fluorouracil, sodium chloride. The prepared medicament can be used for treating tumor.
CN1839951A Anticancer analgesic medicine composition and its preparation method The invention relates to a pharmaceutical composition for anticancer and easing pain, and process for preparation, wherein the composition is prepared from the effective portions and constituents of morphine, Chinese angelica root, goldthread root, banksia rose and borneo camphor through refining, purifying, dissolving with base material, high speed shearing, ultramicro emulsifying, and liquefying with the dissolved base material.
US20090311346 Method for treating acne A novel method for treating acne in an affected area of skin where the method includes having application steps for preparing the affected area of skin, cleansing the affected area of skin and protecting the affected area of skin. The method includes determining a sensitivity level and an irritation level of the affected area of skin to calculate several time periods for applying various cleansers, blends, and lotions to maximize results dependent upon the user's condition.
WO2009120733A1 Pyrrolidine fused indolobenzadiazepine hcv ns5b inhibitors The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
US8846609 Leukotoxin E/D as a new anti-inflammatory agent and microbicide The present invention relates to methods for preventing or treating Human Immunodeficiency Virus (HIV) infection, inflammatory conditions, and graft-versus-host-disease (GVHD) in a subject. Therapeutic compositions of the present invention comprise Leukocidin E (LukE) and/or D proteins or polypeptides. The invention further relates to methods of treating Staphylococcus aureus infection by administering a composition comprising a CCR5 antagonist or any molecule that blocks LukE/D interaction with CCR5+ cells in an amount effective to treat the S. aureus infection in the subject.
CN103070896A Medicine for curing liver-qi stagnation type tumourous fever The invention relates to a medicine for curing liver-qi stagnation type tumourous fever. The medicine is composed of radix bupleuri total saponins, paeoniflorin, aurantiamarin and toosendanin. The medicine has obvious curative effect in curing liver-qi stagnation type tumourous fever, and has no side effect.
US20060135567 Comprehensive pharmacologic therapy for treatment of obesity The comprehensive pharmacologic therapy for treatment of obesity is a procedure which involves the administration of a desired therapeutic range of Diethylpropion and/or Phentermine in combination with a SSRI medication and nutritional supplementation for brief and long durations which may be 12 months or more. The preferred procedure involves the administration of drugs in combination which are identified as: Citalopram (Celexa) and Phentermine; Citalopram (Celexa) and Diethylpropion; Citalopram (Celexa), Phentermine, and Diethylpropion. In addition nutritional supplementation such as a multivitamin, 5-Hydroxytryptophan, vitamin B6, vitamin C, Tyrosine, Calcium, and Lysine may be used to enhance the performance of the weight loss treatment program.
CN101810573A Diammonium glycyrrhizinate microemulsion and preparation process thereof The invention discloses diammonium glycyrrhizinate microemulsion and a preparation process thereof, providing a microemulsion preparation for patients with viral hepatitis. The diammonium glycyrrhizinate microemulsion is prepared from a medical raw material and three auxiliary materials; and the preparation method of diammonium glycyrrhizinate microemulsion comprises a step of preparing auxiliary material solution, a step of preparing raw material solution and a step of preparing microemulsion. The preparation method of diammonium glycyrrhizinate microemulsion is scientific and novel; the preparation process is simple and convenient; the diammonium glycyrrhizinate microemulsion has more functions of non-specific anti-inflammatory, anti-allergy, stable effect on lysosome membrane and immunoregulation in clinical application; in addition, the diammonium glycyrrhizinate microemulsion improves the thermodynamic activity, prevents the first-pass effect of liver and is easier to work. Compared with the other diammonium glycyrrhizinate oral liquid preparations, the diammonium glycyrrhizinate microemulsion has higher bioavailability and more remarkable efficiency of antiviral therapy and is more convenient for patients, who have difficulty to swallow solid medicine.
WO2013093655A1 Non-enteric pharmaceutical composition comprising crofelemer Non-enteric pharmaceutical composition for oral administration comprising crofelemer and a pharmaceutically acceptable excipient is disclosed. The process for preparing such composition and its use in treating secretory diarrhea in a subject are also disclosed.
WO2009114098A3 Methods of treating hyperacidic disorders The present invention relates to methods for treating or preventing hyperacidic disorders such as GERD or NERD using calcium receptor active compounds.
WO2005058932A1 Tear layer stabilizer The invention aims at finding remedies for dry eye or corneal and conjunctival epitheliopathies caused by dry eye. Eye drops containing mannose exert excellent ameliorative effects on dry eye or corneal and conjunctival epitheliopathies caused by dry eye through the stabilization of the tear layer.
WO2012095469A1 Novel heterocyclic derivatives and their use in the treatment of neurological disorders The invention relates to novel heterocyclic compounds of the Formula (I), in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
US20120189537 Nitrile derivatives and their pharmaceutical use and compositions Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.
CN103462974A Application of Incarviatone A in medicaments for treating ovarian cancer The invention discloses an application of Incarviatone A in preparation of medicaments for treating ovarian cancer, and belongs to the technical field of a new application of medicaments. In-vitro methyl thiazolyl tetrazolium (MTT) anti-tumor activity evaluation discovers that the Incarviatone A has a prominent inhibiting effect on growth of human ovarian cancer cell strains HO-8910, HOC1 and OVAC. Therefore, the Incarviatone A can be used for preparing anti-ovarian cancer medicaments, and has a good development and application prospect. The application of the Incarviatone A in preparation of the medicaments for treating the ovarian cancer is made public for the first time, the skeleton type is completely novel, and the Incarviatone A has an unexpectedly strong human ovarian cancer cell inhibiting activity.
WO2013171289A1 Combination of cd37 antibodies with further agents The present invention relates to immunotherapies that are based on depletion of CD37- positive cells such as B-cells. The present invention provides methods for reduction of CD37-positive cells such as B-cells in an individual/ patient using a combination of CD37 antibody /antibodies and bendamustine. The combination of CD37 antibodies, CD20 antibodies and bendamustine is shown to have a synergistic effect. The application further provides materials and methods for treatment of diseases involving aberrant B-cell activity.
US20100247653 Nanoparticles containing nicotine and/or cotinine, dispersions, and use thereof The present invention relates to nanoparticles containing nicotine and/or cotinine. The present invention further relates to dispersions containing these nanoparticles. The invention relates in particular to corresponding novel transdermal pharmaceuticals containing nicotine and cotinine in nanoparticulate form, and use thereof for smoking cessation.
WO2009076408A2 3 -carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): (I) wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
US20090156666 Novel compositions and use thereof for the treatment, co-treatment or prevention of inflammatory disorders The present invention relates to novel compositions comprising magnolol and/or honokiol and glucosamine as well as to the use of these compositions as a medicament, in particular as a medicament for the treatment, co-treatment or prevention of inflammatory disorders.
EP1599206A4 Aminocyclopentyl fused heterotricylicamide modulators of chemokine receptor activity The present invention is directed to compounds of formulae (I and II) (wherein A, D, E. X, l, m, n and R1 through R18 are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
US20060247240 Method of treatment and/or prevention of brain, spinal or nerve injury The invention relates to a method of treatment and/or prevention of brain, spinal or nerve injury comprising administration to a person in need of such treatment, of a therapeutically effective amount of an NK-1 receptor antagonist compound of the formula wherein the meanings of R, R1, R2, R2, R3, and R4 are explained in the specification and the pharmaceutically acceptable acid addition salts and the prodrugs thereof either alone or in combination with a magnesium salt. Exemplified is the use of N-(3,5-bis-trifluoromethyl-benzyl)-N-methyl-6-(4-methyl-piperazin-1-yl)-4-o-tolyl-nicotinamide. The invention also relates to pharmaceutical composition comprising one or more such NK-1 receptor antagonists, optionally in combination with a magnesium salt, and a pharmaceutically acceptable excipient for the treatment and/or prevention of brain, spinal or nerve injury.
US6855835 Allomorph of isomer Z hydrochloride of alkylaminofurane derivative Allomorph of Z isomer of N-[2-[[[5-(dimethylamino)methyl-2-furanyl]methyl]thio]ethyl]-N′-methyl-2-nitro-1,1-ethenediamine hydrochloride, with two carbon atoms linked by a rigid ethylenic bond, marked by an asterisk (*), characterized by the following structural formula: wherein -Fur- represents a furane ring.
CN102085176A Nanometer itraconazole external preparation and preparation method and use thereof The invention provides a nanometer itraconazole external preparation and a preparation method and a use thereof, and the nanometer itraconazole external preparation comprises components of nanometer itraconazole and a matrix, wherein the matrix is selected from the multiple components of octodecyl alcohol, cetyl alcohol, stearic acid, isostearic acid, glyceryl monostearate, white vaseline, sodium lauryl sulfate, glycerin, liquid paraffin, solid paraffin, tween-80, tween-60, span-60, span-80, polyethylene glycol 4000, polyethylene glycol 400, polyethylene glycol 200, carbomer, propylene glycol, ethanol, benzyl alcohol, triethanolamine, carboxylation methyl cellulose, EDTA (ethylenediamine tetraacetic acid) or methyl hydroxybenzoate, and the content of the nanometer itraconazole is 0.1% by weight-10% by weight. By adopting the nanometer itraconazole external preparation, the shortcomings that the itraconazole is difficult to absorb in the external preparation, the skin penetration is not high and the percutaneous absorption rate of the itraconazole is not high are solved, the hepatotoxicity of the itraconazole during metabolism process of a human body is avoided, the bioavailability is improved, and a new administration way is provided for a patient.
US20060248601 Modification of organelle metabolism by unc-51-like kinases roma1 or 2tm proteins The invention discloses polypeptides (Unc-51 kinase, ROMA1, and/or 2TM protein) affecting the activity of Uncoupling Proteins (UCPs), thereby leading to an altered mitochondrial activity and thus contributing to membrane stability and/or function of organelles, preferably mitochondria. This invention relates to the use of these polypepetides in the diagnosis, study, prevention, and treatment of diseases and disorders, for example, but not limited to, metabolic diseases such as obesity, adipositas, eating disorders, wasting syndromes (cachexia), pancreatic dysfunctions (for example diabetes), disorders related to ROS production, and others.
CN101372490B Penem derivative containing sulfhydryl nitrogen heterocyclic ring and vinyl nitrogen heterocyclic ring The invention belongs to the technical field of medicine, and more particularly relates to ertapenem derivatives which are shown in general formula (I) and contain hydrosulphonyl nitrogen heterocyclic ring ethylene azacyclonol, salt which can be accepted by the derivatives on pharmacy, ester of the derivatives that is easy to hydrolyze, and isomer of the derivatives; wherein, R1, R2, R3, R4, m, nand are defined as instruction; the invention also relates to a method used for preparing the compounds, medicine combinations containing the compounds, and the application of the compounds in the preparation of the medicine for treating and/or preventing infectious diseases.
CN102936252A Sesterterpine compounds, and preparation method and application thereof The invention discloses sesterterpine compounds, and a preparation method and an application thereof. The sesterterpine compounds are compound 1, compound 2, and compound 3. The structural formula is represented as the formula (I). The sesterterpine compounds provided by the invention can be used for preparing acetylcholinesterase inhibitor medicines, wherein the medicines can be used for treating senile dementia. The compound 1 is represented as the following. In the compound 2, R1=H, and R2=OH. In the compound 2, R1=H, and R2=OAc (I).
WO2007131154A3 Using naltrexone as a multi-purpose health supplement to improve the human condition and preventing multiple diseases and infirmities by stimulating immune system vitality and robustness Naltrexone has been used to fight existing infections, afflictions, and substance abuse. Embodiments of the current invention provide naltrexone as a preventative medicine taken daily, usually in the late evening for greater efficacy. It is taken in a low dose like a vitamin supplement and may prevent many diseases by stimulating the immune system. The increased endorphin levels resulting from the use of low dose naltrexone may also reduce the need for pain relief medications, plus counter tendencies toward experiencing undesirable moods, such as depression or anger. Increased feelings of well-being produced by naltrexone may also have far- reaching effects, as suggested by studies showing that people with positive attitudes recover more quickly from serious illnesses, for example. In another aspect of the invention, naltrexone may be used to prevent substance addiction before it ever starts, by blocking the internal positive response that normally results from the use of chemical substances.
US7395112 Method and apparatus for treating tumors using low strength electric fields A method of treating tumor tissue of an individual is provided. The method is effected by applying to cells of the tumor tissue electrical field pulses having a strength, a repetition frequency and a pulse width selected capable of inducing endocytosis mediated cell death thereby treating the tumor tissue.
US20110171156 Topical Scar Treatment Composition An anhydrous topical scar treatment product having a water activity of less than 0.50, the product being comprised of (i) a silicone elastomer, (ii) a non-volatile, anhydrous carrier vehicle, (iii) L-ascorbic acid in the form of fine powder, at a concentration of concentration of from 7.5% to 15% by weight, based on the total weight of the anhydrous topical scar treatment product, and (iv) an oil-soluble Vitamin C derivative at a concentration of from 5% to 10% by weight, based on the total weight of the anhydrous topical scar treatment product.
CN102070723A Agaricus bisporus polysaccharide with immunological activity as well as preparation method and application of agaricus bisporus polysaccharide The invention relates to agaricus bisporus polysaccharide with immunological activity. The agaricus bisporus polysaccharide is heteropolysaccharide consisting of ribose, rhamnose, arabinose, xylose, mannose, glucose and galactose, wherein the mole mass ratio of ribose to rhamnose to arabinose to xylose to mannose to glucose to galactose is 2.08:4.61:2.45:22.25:36.45:89.22:1.55. The preparation method comprises the following steps: carrying out water bath on agaricus bisporus; carrying out ethanol precipitation on extract with ethanol; carrying out deproteinization on ethanol sediments by using a Sevag method; performing ion exchange column chromatography on the obtained crude polysaccharose anion exchange padding; eluting with distilled water, and freeze-drying; and carrying out gel chromatography, eluting with distilled water, and freeze-drying, so as to obtain the agaricus bisporus polysaccharide. The polysaccharide has the characteristic of immunologic enhancement, can be used as an adjuvant therapy medicament for hypoimmunity diseases such as tumour or used as functional health care products and foods which have the effect of improving the immunity.
EP1480646B1 Anti-infective agents and/or immunomodulators used for preventive therapy following an acute cerebrovascular accident The invention relates to agents used for preventive therapy following an acute cerebrovascular accident, particularly with the goal of preventing infections following a cerebrovascular accident. According to the invention, the agents used in pharmaceutical preparations are anti-infective agents and/or immunomodulatory agents, for example, cytokines and/or inhibitors of the sympathetic nervous system.
CN103550775A Anti-insomnia composition, application of composition, multi-phase pulse immediate-release preparation prepared by use of composition and preparation method of preparation The invention discloses an anti-insomnia composition, an application of the composition, a multi-phase pulse immediate-release preparation prepared by use of the composition and a preparation method of the preparation. The anti-insomnia composition consists of a component A and a component B, wherein the component A is one or more of melatonin, melatonin analogue and corresponding salt, melatonin receptor stimulant, 5-hydroxytryptamine 2C, receptor antagonist and 5-HTP (5-hydroxytryptophan); the component B is one or more of petroselinum neapolitanum extract, melissa extract, tuber fleeceflower stem extract, chamomile extract, passion flower extract, radix paeoniae alba extract, manyprickle acanthopanax extract, polygala tenuifolia extract, hyperforin perforatum extract, flos albiziae extract, lily extract and prunella vulgaris extract. The composition and the multi-phase pulse immediate-release preparation prepared by use of the composition have the characteristic of better anti-insomnia effect than a common melatonin preparation, and can effectively solve and improve the problem of difficult sleep of human or mammals while effectively solving and improving the insomnia problems such as light sleep or dreaminess or early awakening or difficult sleep after wakeup of human or mammals.
WO2011153502A3 Anti-inflammatory and quorum sensing inhibition compounds and methods of making and using them The invention provides novel compositions based on a structure designated as "Honaucin A", including Honaucin A variants and analogs, and pharmaceutical compositions, liposomes and nanoparticles comprising them, and methods of making and using them. In one embodiment, these Honaucin A compounds, and variants and analogs thereof are used to ameliorate (including to treat or prevent) inflammation. In one embodiment, these Honaucin A compounds, and variants and analogs thereof are used to ameliorate (including to treat or prevent) inflammation. In one embodiment, these Honaucin A compounds, and variants and analogs thereof are used as bacterial quorumsensing inhibitors. Accordingly, in alternative embodiments the compositions of the invention are used as anti-bacterial agents.
CN102718977A Heparin sodium-loaded polyurethane micro nanometer particle solution and preparation method and application thereof The invention aims to provide a heparin sodium-loaded polyurethane micro nanometer particle solution with a controllable particle size and a preparation method thereof. The preparation method comprises the following steps: dissolving polyurethane with a mixed solvent of tetrahydrofuran and acetone in the volume ratio of 1:4-4:1, so that the concentration of the polyurethane is 0.01-1%; while rapidly stirring, adding an equal volume of sodium heparin aqueous solution with the concentration of 0.01-1%, and thus obtaining a crude product; and putting the crude product into a dialysis bag, and dialyzing in deionized water to remove organic solvents of tetrahydrofuran and acetone and free sodium heparin, and thus obtaining the heparin sodium-loaded polyurethane micro nanometer particle solution having a particle size of 500-1500nm. The preparation method is simple in process route, low in energy consumption and free of pollution and provides an idea for safer and more effective clinical application of an anticoagulant medicine heparin sodium and preparation of polyurethane-based novel composite material.
CN102784109A Taxane medicines albumin nanoparticle preparation for injection and preparation method thereof The invention belongs to the field of medicinal preparation, and relates to taxane medicines albumin nanoparticle preparation for injection and a preparation method of the preparation. According to the invention, the albumin nanoparticle preparation is prepared by combining the albumin with the taxane medicines to form the albumin nanoparticles by dispersing and stabilizing with the phospholipid. According to the invention, the strengthened osmosis and retention effect on the tumors by the nanoparticles are utilized, and more medicines are passively targeted and concentrated on the tumor tissues so as to improve the antitumor effect; simultaneously, due to the fact that the bioavailability in the injection way is high and the soluble albumin nanoparticle preparation for injection exists passive targeting, the administration dose can be greatly reduced, so that the medicinal concentration on the non-target parts can be effectively reduced, the toxic and side effects of the medicines can be reduced, and the good clinical application prospect can be implemented. The preparation is convenient in preparation method and is suitable for industrial mass production.
US20110166156 Prodrugs for the Treatment of Schizophrenia and Bipolar Disease Compounds of Formula I and Formula II and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed.
WO2009037001A3 Novel tetrahydrofusedpyridines as histone deacetylase inhibitors The compounds of formula (I), wherein ring D and ring E together form a fused ring system selected from formula (II), (III), (IV), (V), (VI), (VII), and the salts of these compounds are novel, effective inhibitors of histone deacetylases.
CN101724039A Human epididymal expression sperm binding protein HEL-38 as well as encoding gene and application thereof The invention belongs to the biotechnology and the medical field and discloses a new human epididymal specific expression sperm binding protein HEL-38 as well as preparation and application thereof. The invention discloses an amino acid sequence of the HEL-38 protein and provides a recombinant expression vector which carries a DNA sequence used for encoding the protein. The protein is located at the main section region and the terminal segment region of the tail of a mature sperm, and the gene mainly has specific expression in an epididymis, indicated by RT-PCR. A band of about 35 KD is detected in the epididymis by using Western blot. The HEL-38 protein can be used as a target protein for developing an immunological contraceptive and clinically diagnosing and treating male infertility. A method for detecting a corresponding gene or protein based on development of the HEL-38 protein can be widely used for the research field of reproductive medicine.
CN102716109A Application of glycine to preparation of medicine for treating AD (alzheimer diseases) The invention relates to a purpose of glycine, in particular to an application of glycine to the preparation of medicine for treating AD (alzheimer diseases), which solves the problem of lack of effective medicine for treating AD and provides medicine for effectively preventing and treating AD. AD mice with high-fructose diet or intraperitoneal galactose injection and AlCl3 induction are adopted for experiments, the damaged memory function of the mice can be effectively improved through the oral administration of the glycine, and the Abeta1-40 level in the brain, the number of age pigment and the abnormal phosphorylation expression of Tau protein are reduced. The results show that the glycine has the obvious prevention and treatment effect on AD and can be widely applied to the medicine for treating AD.
US20070218057 Human Obesity Susceptibility Gene and Uses Thereof The present invention discloses the identification of a human obesity susceptibility gene, which can be used for the diagnosis, prevention and treatment of obesity and related disorders, as well as for the screening of therapeutically active drugs. The invention more specifically discloses that the MAP3K11 gene on chromosome 11 and certain alleles thereof are related to susceptibility to obesity and represent novel targets for therapeutic intervention. The present invention relates to particular mutations in the MAP3K11 gene and expression products, as well as to diagnostic tools and kits based on these mutations. The invention can be used in the diagnosis of predisposition to, detection, prevention and/or treatment of coronary heart disease and metabolic disorders, including hypoalphalipoproteinemia, familial combined hyperlipidemia, insulin resistant syndrome X or multiple metabolic disorder, coronary artery disease, diabetes and dyslipidemic hypertension.
WO2009093210A3 SUBSTITUTED CYCLOALCANO[e AND d] PYRAZOLO [1,5-a]PYRIMIDINES/ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS AND METHODS FOR PRODUCTION AND THE USE THEREOF The invention relates to antagonists of serotonin 5-HT6 receptors / substituted 2-alkylsulfonyl-3-arylsulfonyl-cycloalcano[e and d] pyrazolo[1,5-a]pyrimidines, to novel medicinal principles and pharmaceutical compositions which contain the medicinal principles in the form of the above-mentioned compounds, to novel medicinal agents and to a method for treating and preventing the development of CNS diseases in human beings and warm-blood animals, the pathogenesis of which is depends on 5-HT6 receptors. In general formulas (1) and (2) : R1 is a hydrogen atom or C1-C3 alkyl; R2 is C1-C3 alkyl; R3 is a hydrogen atom, one or two optionally the same halogen atoms, C1-C3 alkyl and optionally alkyl-substituted hydroxyl; and n is an integer 1, 2 or 3.
CN101214221A Pharmaceutical formulation for treating rhinitis and sinusitis A medical preparation for remedying rhinitis and sinusitis is a preparation of an ointment or aqua for partial application, which is made by stirring and mixing matrix and antifungal drug uniformly. The drug can directly act on an affected part by the partial application method of being coated or dripped into a nasal cavity to effectively remedy the rhinitis and the sinusitis, which not only has obvious curative effect and 100 percent of effective rate but also has no toxic and side effect and bad reaction.
CN1872087A Medication of possessing function of anti inflammation, for improving rheological property of blood, and restraining thrombosis A kind of 4 anti-inflammatory medicines for improving the rheological property of blood, suppressing thrombosis and treating inflammatory arthritis is prepared proportionally from Sailaixibu, sodium selenite and dipyridamole.
WO2009020198A1 Aniline derivative having anti-dna virus activity How virus-infected patients are treated has become more of a serious issue accompanying an increase in compromised hosts such as cancer patients, organ transplant patients, and AIDS patients. Further, the development of an effective anti-virus compound against a virus showing resistance to existing drugs has been strongly demanded. The invention provides a novel anti-DNA virus agent and a method of using the same. Further, the invention provides an anti-DNA virus agent effective also in a drug-resistant virus and a method of using the same.
US20110021546 Gene Defects And Mutant ALK Kinase In Human Solid Tumors In accordance with the invention, novel gene deletions and translocations involving chromosome 2 resulting in fusion proteins combining part of Anaplastic Lymphoma Kinase (ALK) kinase with part of a secondary protein have now been identified in human solid tumors, e.g. non-small cell lung carcinoma (NSCLC). Secondary proteins include Echinoderm Microtubule-Associated Protein-Like 4 (EML-4) and TRK-Fusion Gene (TFG). The EML4-ALK fusion protein, which retains ALK tyrosine kinase activity, was confirmed to drive the proliferation and survival of NSCLC characterized by this mutation. The invention therefore provides, in part, isolated polynucleotides and vectors encoding the disclosed mutant ALK kinase polypeptides, probes for detecting it, isolated mutant polypeptides, recombinant polypeptides, and reagents for detecting the fusion and truncated polypeptides. The disclosed identification of this new fusion protein enables new methods for determining the presence of these mutant ALK kinase polypeptides in a biological sample, methods for screening for compounds that inhibit the proteins, and methods for inhibiting the progression of a cancer characterized by the mutant polynucleotides or polypeptides, which are also provided by the invention.
WO2006065853A3 Crystalline forms of a factor xa inhibitor The instant invention provides crystalline forms of 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one and its solvates thereof; processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.
WO2013072520A1 N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy The present invention relates to N-substituted aminobenzocycloheptene,aminotetraline, aminoindane and phenalkylamine derivatives of the formula (I),(II), (III) or (IV) or a physiologically tolerated salt thereof. The invention relates topharmaceutical compositions comprising such N-substituted amino-benzocycloheptene,aminotetraline, aminoindane and phenalkylamine derivatives, and the use of such N-substituted aminobenzocycloheptene,aminotetraline, aminoindane and phenalkylamine derivatives for therapeutic purposes. The N-substituted aminobenzocycloheptene,aminotetraline, aminoindane and phenalkylamine derivatives are GlyT1 inhibitors.
WO2008110697A3 Use of a compound antagonist to the nk2 receptors of a neurokinine for the preparation of drugs useful for preventing and treating sexual dysfunction The invention relates to the use of a compound antagonist to the NK2 receptors of A neurokinine for the preparation of drugs useful for preventing and treating sexual dysfunction.
US20110081317 Enhancing Gene Transfer Described herein are methods of improving the efficiency of gene transfer for a wide range of applications. Specifically provided are methods of increasing expression of an exogenous gene in a cell by contacting the cell with a vector comprising the exogenous gene and contacting the cell with a proteasome inhibitor, a lysosomal protease inhibitor and/or a microtubule inhibitor. Also provided are methods of delivering an antigen delivery vector to a cell or a subject. Provided are antigen delivery systems and kits comprising an antigen delivery vector and a proteasome inhibitor, a lysosomal protease and/or a microtuhulc inhibitor.
CA2709132A1 Target host factors for treating viral infection A method of reducing virus-mediated cytotoxicity comprising contacting virus-infected cells with an effective amount of at least one inhibitor of ABI2, ARRDC3, BAD, BRCA1, C17orf85, C1orf71, C6orf162, CCNJL, CFL1, GON4L, HCG 1986447, HIST1H2AB, HPS4, LHX8, RPS25, RPL23, RPL32, LOC730139, LRRC39, MALT1, MX1, MERTK, MX2, NRG1, OR52A1, PLEKHH1, PTPN13, PTPRJ, RLN1, RNF19A, SH3BP4, SLC7A14, ST8SIA3, STX3, TMC6, TMTC4, TNFSF12-TNFSF13, TNFSF13, TTN, UBXN7, USP47, WNK2, YPEL2, ZNF251 and/or SCG2.
CN102579463A Application of glibenclamide compound in preparation of information therapy medicament, method for preparing information therapy medicament, and novel drug prepared with method The invention discloses an application of a glibenclamide compound in preparation of an information therapy medicament, a method for preparing the information therapy medicament, and a novel drug prepared with the method. The information therapy medicament is not in direct contact with a human body during treatment, the components of the medicament is not consumed, only medicament information is utilized for physical therapy, so that the chemical treatment effect can be achieved, the therapeutic window is enlarged by more than a thousand times, and the side effect of chemical treatment is avoided. After the glibenclamide is used as the information therapy medicament, the content of effective components of the glibenclamide is not changed, so that the glibenclamide can be used as a conventional preparation in chemical treatment for secondary effective use.
EP1334086B1 Phenoxyphenyl alkane sulfonates The invention relates to phenoxyphenyl alkane sulfonates of the formula (I), wherein A represents oxygen or NH, and R<3> represents (C4-C7) alkyl that can be mono- or polysubstituted by fluorine or chlorine. The invention further relates to methods for producing the same, to the use of said sulfonates in the production of medicaments for the treatment and/or the prophylaxis of diseases, especially for treating pain conditions and neurodegenerative diseases.
WO2012011875A1 Compounds for photodynamic therapy A metal-ligand complex comprising a transition metal complexed with at least one Schiff base ligand comprising an additional nitrogen atom from a heterocycle and at least one heteroaromatic nucleic acid intercalating moiety. A pharmaceutical composition comprising the compound in admixture with a pharmaceutically acceptable carrier togther with use of the compound in the treatment of cancer, macular degeneration, human papilloma virus (HPV) warts and a skin disorder is also provided.
WO2014006576A1 Pharmaceutical compositions comprising rifaximin and amino acids, preparation method and use thereof The object of the present invention concerns rifaximin compositions comprising amino acids, characterized in that they increase rifaximin solubility in aqueous solutions. Rifaximin compositions comprising amino acids are useful in the treatment of disease wherein amino acids and rifaximin are efficacious. The present invention relates to pharmaceutical compositions comprising rifaximin or one of the pharmaceutically acceptable salts thereof and one or more amino acid(s), wherein the molar ratio between the amino acid(s) and rifaximin is comprised between 1:1 and 10:1, preferably between 1:1 and 5:1, together with pharmaceutically acceptable excipients. Moreover, the present invention relates to rifaximin crystals characterized in that they are obtained by means of a process comprising: a) dissolution of the compositions of rifaximin and amino acids, wherein amino acids and rifaximin are in a molar ratio comprised between 1:1 and 10:1 according to Claim 1, in solutions formed by ethanol/water, in a volumetric ratio comprised between 1:1 and 1:10 (v/v); b) evaporation of the solution obtained in step a) at temperatures comprised between room temperature and 40°C, in a time period comprised between 1 and 10 days; wherein the resulting crystals have monoclinic space group P21 and cell parameters comprised in the ranges: a: 13.7(1)-13.8(1) Å; b: 19.7(1)-19.9 (1) Å; c: 16.4(6)-16.6(6) Å; β: 92.1 (1)-91.9(1) deg.
US20090036389 Polymeric Micelle Formulations of Hydrophobic Compounds and Methods Provided are cosolvent evaporation methods and compositions for improving the solubility of hydrophobic compounds, including therapeutic agents such as anticancer drugs, polyene antibiotics, antilipidemic agents, and hydrophobic compounds used in various industries, and/or for reducing the toxicity of certain hydrophobic therapeutic agents, especially polyene antibiotics, in particular, Amphotericin B (AmB), and therapeutics such as paclitaxel, tamoxifen, an acylated prodrug or an acylated cis-platin, by incorporating these agents within micelles comprising an amphiphilic block-forming copolymer.
US20110052602 Diagnosis and Treatment of Age Related Macular Degeneration Methods, compositions and kits for diagnosis and treatment of age related macular degeneration.
CN101700230A Monosialote rahexosylganglioside microsphere and preparing method thereof The invention discloses a monosialote rahexosylganglioside (GM-1) microsphere, comprising monosialote rahexosylganglioside, carrier material, emulsifier and water, wherein the concentration of the components is: monosialote rahexosylganglioside 80 to 240 mg/ml, carrier material 20 to 200 mg/ml and emulsifier 10 to 50 mg/ml. The monosialote rahexosylganglioside microsphere of the invention can be used for injection and has uniform quality and appearance, with the average grain diameter being 1 to 15 microns and the encapsulating rate higher than 80%. The monosialote rahexosylganglioside microsphere has obvious slow release function, obviously decreases the dose times and increases the adaptation of sufferer.
US20110288069 Benzodiazepine and Pyridodiazepine Derivatives The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
US20100222380 Modified Chalcone Compounds as Antimitotic Agents Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN-COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an α,β-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.
CN102895220A Ketoprofen intravenous administration preparation and preparation method thereof The invention provides a ketoprofen intravenous administration preparation and a preparation method thereof. The injection contains 0.4mg / ml-4mg / ml ibuprofen, an alkali modifier in the amount required for adjusting pH to 6.5-9.0, 0.70%-0.90% w / v sodium chloride and water for injection.
CN101450912B Tetrahydronaphthalene substituted benzoic acid derivates The invention belongs to the technical field of medicine, in particular to tetraline substituted benzoic acid derivatives shown in the general formula (I), pharmaceutically acceptable salts or isomers thereof, wherein R<1>, R<2>, R<3>, R<4>, R<5>and R<6>are defined as the description. The invention also relates to a method for preparing the compounds, medical compositions containing the compounds, and application of the compounds in preparing medicines for treating and/or preventing infectious disease.
WO2010099169A2 A novel in vitro hiv-1 latency model for screening reactivation agents of hiv-1 In one aspect, the present invention provides an isolated Bcl-2-transduced cell that comprises, integrated into the genome of the cell, a transcription-competent immunodeficiency virus or a transcription-competent immunodeficiency virus-based retroviral vector. Under basal in vitro culture conditions, the immunodeficiency virus is latent, and the expression of the latent immunodeficiency virus can be reactivated. The present invention further provides screening methods for identifying agents capable of reactivating latent immunodeficiency virus or blocking the reactivation of latent immunodeficiency virus. In another aspect, the present invention provides such identified agents and methods for treating subject having an immunodeficiency virus infection.
WO2005077381A1 Use of ginsenoside re for preparation of medicaments for treating dysmnesia Use of ginsenoside re for preparation of medicaments for treating dysmnesia, dysmnesia, improving ß-amyloid peptide induced spatial identification disease, and promoting the basic synaptic transmission, and facilitating the formation of LTP.
US7378107 administering triglycerides such as triester of caprylic acid or capric acid with glycerin, used along with foods or drugs, without concerning about side effects and restrictive diets The present invention discloses serum remnant-like lipoprotein concentration regulators containing triglyceride of medium-chain fatty acids, wherein 90% or more by weight of the fatty acids as components of the medium-chain triglyceride are saturated fatty acids having 8 and 10 carbon atoms; weight ratio between the saturated fatty acids having 8 carbon atoms and those having 10 carbon atoms is 60/40 to 85/15; and the proportion of the saturated fatty acids having 8 carbon atoms in all the fatty acids bonding to the second position of the triglyceride is 60 to 85 % by weight. The present invention also discloses foods for controlling the concentration of serum remnant-like lipoproteins and pharmaceutical compositions for controlling the concentration of serum remnant-like lipoproteins, which contain the serum remnant-like lipoprotein concentration regulator. The foods for controlling the concentration of serum remnant-like lipoproteins can be easily used without concerning about side effects and restrictive diet.
CN101671346B Lindenrane-type dimerization sesquiterpenoids, preparation method and applications thereof in pharmacy The invention relates to a lindenrane-type dimerization sesquiterpenoids (structural format I and II) separated from chloranthus plant, a preparation method and applications thereof on medicament in curing type 2 diabetes mellitus, adiposity and other complications caused thereby. In the formula I and II, R1-R17 is hydrogen or oxygen or hydroxy group or acyl (acetyl, angelica acyl, hydroxyl angelica acyl, tigloxyl, senecioyl, hydroxyl senecioyl, carboxyl senecioyl and 1, 4-carboxybutyryl group) or double bond or alkyl (methyl) or macrolide can be formed between R16 and R17, wherein X is oxygen or nitrogen. The biological experiment proves that the compound has stronger insulin-sensitizing activity.
CN102552164A Potassium citrate slow-release micro pill and preparation method thereof The invention belongs to the field of medicament preparation, and discloses a potassium citrate slow-release micro pill and a preparation method thereof. The micro pill is formed by wrapping slow-release coating materials on a medicine-containing pill core, wherein the prescription of the medicine-containing pill core contains potassium citrate 75-100 parts by weight and excipient 0-25 parts by weight. The sum of the parts of the potassium citrate and the excipient is 100 parts by weight, or the parts of the potassium citrate and the excipient are enlarged or minimized with equal ratio, a surface active agent is 0.1-8% of the sum of the weight of the potassium citrate and the excipient, and a moisture agent is 0.1-30% of the sum of the weight of the potassium citrate and the excipient. By means of the method, the medicine-containing pill core with low breakage, high yield, small particle size and a smooth and clean surface can be obtained, and the pill core facilitates further processing. The potassium citrate slow-release micro pill is formed by wrapping the slow-release coating materials on the medicine-containing pill core, the micro pill has the advantages that the quality is controllable and stable externally, and the micro pill can be slowly released internally.
US8536164 Fused pyridine compounds as casein kinase inhibitors Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
WO2008121066A1 Novel tricyclic spiropiperidines or spiropyrrolidines and their use as modulators of chemokine receptors The present invention relates to new compounds of formula (I) or salts, solvates or solvated salts thereof, wherein Q, X, Y, Z, R1, R2, R3, R4 and m, n and p are defined as in claim 1, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions comprising said compounds and to the use of said compounds as modulators of chemokine receptor activity in the treatment of airway diseases, inflammatory diseases, COPD and asthma.
US20050038060 Spiropoperidine compounds as ligands for orl-1 receptor A compound of the formula (I) or a salt, prodrug or solvate thereof, wherein R1 and R2 groups are all hydrogen; A is a benzofuzed azahetero ring; W1—W2 is CH2—CH2; X1—X1 is CH2—CH2; and Z is methylene or carbonyl; or the like, is a ligand for ORL1-receptor and are useful for treating or preventing pain, a CNS disorder or the like in mammalian subjects.
WO2005021038A3 Agent for treating metabolic syndrome The invention relates to an agent for treating metabolic syndrome and comprises at least one weight-reducing compound having a satiating effect and being capable of swelling or forming a gel, at least one cholesterol-lowering substance and/or an antidiabetic agent and optionally an antihypertonic agent. The inventive agent is characterized in that the ratio of the cholesterol-lowering substance to the compound having a satiating effect and/or the ratio of the antidiabetic agent to the compound having the satiating effect ranges between 9:1 and 1:9 if polymers are used as the cholesterol-lowering substance or the antidiabetic agent, and ranges between 1:1000 and 1:20 if pharmaceutically active substances are used as the cholesterol-lowering substance or the antidiabetic agent.
CN103561741A Substituted N-aryl pyridinones Disclosed herein are methods of administering deuterated pirfenidone and kits thereof.
WO2014143609A1 Isoquinolines as potassium ion channel inhibitors A compound of formula (I) (I) wherein A, R1, R1a, R3 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
CA2415396C 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications Compounds of formula (I) are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands. Also disclosed are histamine-3 receptor ligand compositions and methods of antagonizing or agonizing histamine-3 receptors.
EP2741752A2 The utility of nematode small molecules The present invention relates to methods of treating immune disorders and/or inflammation using certain modulator compounds. In one embodiment, the present invention provides a method of treating an immune and inflammatory disorders disorder by administering a composition comprising a therapeutically effective dosage of an ascaroside compound, or a mixture of ascaroside compounds, or a mixture containing at least one ascaroside..
US20100216816 Pyrazinyl amide-t type calcium channel antagonists The present invention is directed to pyrazinyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
EP1202728B1 Peroxovanadium compounds as protein tyrosine phosphatase (ptp) inhibitors: their inhibitory effects on angiogenesis, restenosis and the production of endothelins. The present invention relates to the use of peroxovanadium compounds in the prevention of angiogenesis, restenosis and the production of endothelins, and as immunomodulators. Peroxovanadium compounds are preferred since they are more potent, and less toxic, than their 'oxo' counterparts. Anti-angiogenic activity was verified in vitro against human umbilical vascular endothelial cells (HUVECs) as well as ex ovo using the chicken chorioallantoic assay membrane and in the rat aortic ring model and a Matrigel assay in vivo. Peroxovanadium compounds also decrease basal levels and inhibit the increase in plasma endothelins occurring following insulin induction in rats. It is proposed that peroxovanadium compounds are therapeutically-active anti-angiogenics and useful in preventing vascular restenosis by acting, inter alia, by inhibiting one or several protein tyrosine phosphatases (PTPs) involved in the proliferation, differentiation and migration of cells or the secretion of peptides (such as endothelins and immunomodulators), or both.
US20100173857 Spinosyns For Wound Healing A spinosyn or a physiologically acceptable derivative or salt thereof for promoting or accelerating wound healing in humans.
US8829028 5-HT4 receptor antagonists for the treatment of heart failure This invention provides the use of a 5-HT4 receptor antagonist in the manufacture of a medicament for treating or preventing heart failure. Particular heart disorders to be treated are selected from the group comprising chronic heart failure, congestive heart failure, chronic congestive heart failure and heart failure resulting from ischaemic heart disease. Methods of treating heart failure using 5-HT4 receptor antagonists and pharmaceutical compositions containing 5-HT4 receptor antagonists are also provided.
US6962936 Treating diseases such as cancer, inflammatory disorders, restenosis, Described herein are compounds that are useful as protein kinase inhibitors having the formula: where Ht, R2, T, and m are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
EP2022783A1 "Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors" The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
CN1981870A Invert-sugar powdery injection and its production An invertose powder injection is prepared from glucose and pectose through preparing aseptic pectose, preparing aseptic glucose, sterilizing tubular bottle, sterilizing butyl rubber plug, mixing aseptic pectose with aseptic glucose to become invertose, loading in aseptic tubular bottle, sealing, and packing.
US20120053213 2-(4-substituted phenylamino) polysubstituted pyridine compounds as inhibitors of non-nucleoside hiv reverse transcriptase, preparation methods and uses thereof The invention relates to 2-(4-Substituted phenylamino) polysubstituted pyridine compounds as inhibitors of non-nucleoside HIV reverse transcriptase, preparation methods and uses thereof. Specifically, the invention relates to compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the description. The compounds of formula I of the invention are a type of anti-HIV active compounds having new backbone structure.
CN101721322A Self tanning compositions containing dihydroxyacetone, a retinoid and ascorbic acid glucoside as a stabilizer The invention concerns a composition comprising dihydroxyacetone, A retinoid and a glycosylated ascorbic acid.
CN1846725A Application of licoflavone in preparing medicine for treating inflammatory enteropathy The present invention relates to application of licoflavone in preparing medicine for treating inflammatory enteropathy. Licoflavone can inhibit inflammation reaction and resist oxidation to reach the aim of treating inflammatory enteropathy. The medicine prepared with licoflavone has high curative effect on inflammatory enteropathy, wide safety range and other advantages.
CN101062906A Agmatine sulfate hydrate and usage for drug rehabilitation, antiphlogistic, hypoglycemic and agmatine metabolism abnormality induced disease The invention discloses a guanidine butylamine sulfate hydrate as formula I and medicinal compound and the usages in aspect of drug rehabilitation, antiphlogistic, hypoglycemic and the disease which caused by guanidine butylamine metabolism abnormal.
US20050203127 2-(Phenyl)-2h-pyrazole-3-carboxylic acid-n-4-(thioxo-heterocyclyl)-phenyl-amide derivatives and corresponding imino-heterocyclyl derivatives and relates compounds for use as inhibitors of the coagulation factors xa and/or viia for treating thromboses The invention relates to the novel compounds of formula (I), wherein D, M, W, X, Y, T, R1 and R1′ are defined as in patent claim 1. The inventive compounds are inhibitors of coagulation factor Xa and can be used in the prophylaxis and/or therapy of thromboembolic diseases and in the treatment of tumors.
CN102861081A Application of Houttuynoid C in medicine for treating skin cancer The invention discloses application of Houttuynoid C in preparation of a medicine for treating skin cancer, belonging to the technical field of new application of medicine. The invention discovers that Houttuynoid C has the remarkable inhibitory effects on the growth of human skin cancer cell strains, including A431, HME1, A375 and SK23 through the evaluation of in vitro MTT antineoplastic activity. Therefore, Houttuynoid C can be used for preparing the anti-skin cancer medicine and has good development and application prospects. The application of Houttuynoid C in preparation of the medicine for treating skin cancer provided by the invention is disclosed firstly. The skeleton type belongs to brand new skeleton type, and the inhibitory activity of Houttuynoid C on skin cancer cells is unexpectedly strong.
CN103340833A Fentanyl double-layer buccal tablet and preparation method thereof The invention discloses a fentanyl double-layer buccal tablet and a preparation method thereof. The buccal tablet is composed by a quick release layer (an outer layer) and a sustained release layer (an inner layer) which form a biphasic drug release system. The quick release layer is prepared by effervescence and cyclodextrin inclusion technologies, a transient change of a pH value happens around the tablet by utilizing an effervescence reaction, and the quick release layer rapidly disintegrates and releases fentanyl in a few minutes; the sustained release layer slowly releases drugs to maintain an effective plasma concentration for up to a few hours. The buccal tablet releases the drugs from fast to slow, maintains the effective plasma concentration for a long time, is easy to use, is safe and reliable, and has the characteristics of rapid and continuous analgesia.
WO2007030617A1 Inhibitors of bacterial impdh The present invention relates to methods of inhibiting bacterial IMPDH comprising administering compounds of formula I: or pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infections.
CN103381149A Venlafaxine hydrochloride single-chamber osmotic pump controlled release tablet and preparation method thereof The invention disclosed a venlafaxine hydrochloride single-chamber osmotic pump controlled release tablet and a preparation method thereof, belonging to the field of medicine science and technology. The tablet comprises a single-layer drug tablet core containing venlafaxine hydrochloride and an insoluble semipermeable film with a small hole, wherein the tablet core is composed of venlafaxine hydrochloride, hydroxypropyl methylcellulose, an osmotic pressure promoter, a pharmaceutically-acceptable inert excipient, a binder and a lubricant in a certain ratio, a semipermeable film coating is composed of cellulose acetate and a hole forming agent, and the small hole is perforated in a mechanical or laser boring manner so as to form one or more channels with a certain size in the semipermeable film, thereby forming a single-chamber osmotic pump controlled release system which realizes zero-level release of venlafaxine hydrochloride. The tablet provided by the invention has the advantages of reasonable composition and a good controlled release effect.
CA2169451C Biochemically balanced peritoneal dialysis solutions A peritoneal dialysis solution that is biochemically balanced to correct metabolic acidosis associated with chronic renal failure in a more physiological manner. The peritoneal dialysis solution has a physiological pH, e.g., pH of 7.0 to 7.4, and contains bicarbonate at a that is found in normal blood. Additionally the solution contains carbon dioxide at a partial pressure that is similar to partial pressure of carbon dioxide found in normal blood. The peritoneal dialysis solution also contains a weak acid with a pKa of less than 5Ø
US20050228043 Preparation of trans-fused 3,3a,8,12b-tetrahydro-2H-dibenzo[3,4:6,7]cyclohepta[1,2-b]furan derivatives The present invention concerns processes for the preparation of each of the 4 diastereomers of formula (I) in stereochemically pure form from either of two enantiomerically pure precursors. The tetracyclic ringsystem having trans-fused five and seven membered rings is formed in an acid-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates, the methanamine end-products, the methanamine end-products for use as a medicine, in particular as CNS active medicines.
CN101225389A VR gene order of diffuse large B cell lymphoma related antigen specific TCR V alpha 23 subfamily and uses thereof The invention discloses a nucleotide sequence and the application of an antigen-specific T cell receptor of the diffuse large B cell lymphoma. According to the RT-PCR genescan analysis, the TCR V Alpha 23 subfamilies in the peripheral blood of patients shows an obviously monoclonal state, and the V-N-J region, namely, the complementary determining region 3, where the PCR products conduct the sequence analysis of the specific TCR sequence, is a part recognizably bound to the antigenic specificity; the genescan analysis also indicates that the TCR of the clonal T cell is a specific TCR produced due to the stimulus of the DLBL associated antigens, and is the basis and key for performing DLBL molecular targeted adoptive immunotherapy by means of the TCR transgenic technique. The nucleotide sequence of the specific TCR plays a significant role in further carrying out lymphoma-specific cellular immunotherapy.
CN102688216A Gabapentin tablet and preparation method thereof The invention belongs to the field of medicine preparation and relates to a gabapentin tablet which is prepared by wet granulation and prepared mainly from the following raw materials by weight percentage: 80.0% or more of gabapentin, 4.0-17.0% of low-substituted hydroxypropyl cellulose, 0.5-2.5% of adhesive, 0.1-2.5% of stabilizer and 0.5-1.5% of lubricant. The invention further provides a preparation method of the gabapentin tablet. The gabapentin raw material adopted in the invention has good formability and high physical strength after being crushed. Besides, the gabapentin raw material can be prepared by adopting an ordinary wet granulation method and has the characteristics of simple preparation and low cost. The gabapentin tablet provided by the invention has the advantages of very high dissolution in vitro, high content of gabapentin, less application auxiliary materials and high convenience for use, thus meeting modern medicine's requirements of 'small in three aspects' and 'convenient in three aspects', and can be prepared by adopting an ordinary wet granulation method and has the characteristics of simple preparation and low cost.
CN102526086A Method for extracting ligustroflavone and application of ligustroflavone to preparation of medicines The invention relates to ligustroflavone and application of the ligustroflavone to the preparation of medicines. A method for extracting the ligustroflavone comprises the following steps of: adding turpinia Montana leaves or glossy privet fruit into 30 to 90 percent ethanol in an amount which is 5 to 15 times that of the turpinia Montana leaves or the glossy privet fruit, performing reflux extraction for 1 to 3 times, wherein the reflux extraction time of each time is 1 to 3 hours, and filtering; mixing filtrate, recovering the ethanol, allowing an aqueous solution to pass through a macroporous resin, eluting, collecting an eluted part, concentrating under reduced pressure, and drying to obtain mixed total glycosides of the ligustroflavone; and performing silicagel column chromatography and Sephadex LH-20 column chromatography for separating, mixing ligustroflavone cut fractions, and crystallizing to obtain a ligustroflavone pure product. The ligustroflavone can be used as a neuraminidase inhibitor for preventing and treating influenza and can be prepared into pharmaceutically-acceptable preparations.
US8258272 20-O-beta-D-glucopyranosyl-20(S)-protopanaxatriol; apoptosis promoters, inhibitors; transcription factors; skin aging, cancer The present invention relates to an agent for controlling Bcl-2 expression comprising ginsenoside F1 (20-O-β-D-glucopyranosyl-20(S)-protopanaxatriol) represented by the following formula 1 as an active component.
US20100286243 Mig-7 as a specific anticancer target Aspects of the present invention provide novel Mig-7 encoding nucleic acids and Mig-7 polypeptides, RNAi (such as siRNA), recombinant DNA expression systems and host cells containing same, as well as methods of inhibiting expression of the subject nucleic acid molecules, inhibiting production of the encoded proteins or polypeptides, inhibiting metastasis of a carcinoma cell in a subject (including in humans), inhibiting migration/invasion of and mimicking of normal cells by carcinoma cells in a subject, detecting the presence of a cancer cell (e.g., a migrating/invading cancer cell or carcinoma cell mimic, tumor neovas-cularization, and/or vascular mimicry) in a sample of a subject's tissue or body fluids, and inhibiting the migration/invasion of an endothelial cell mimicking by a placental cell into the blood stream or vessels of a female mammal. Particular aspects relate to novel anti-Mig-7 antibodies, diagnostic and/or prognostic methods, and therapeutic methods comprising use of the inventive nucleic acids, polypeptides and antibodies or derivatives thereof.
EP1135482B1 Cancer cell vaccine Disclosed is a specific regulator of Ii protein expression or immunoregulatory function. Specifically disclosed are several forms of the specific regulator of Ii, including those which function through the formation of a duplex molecule with an RNA molecule encoding mammalian Ii protein to inhibit Ii protein synthesis at the translation level. This class includes copolymers comprised of nucleotide bases which hybridize specifically to the RNA molecule encoding mammalian Ii protein, and also expressible reverse gene constructs. In other aspects, the disclosure relates to MHC class II-positive antigen presenting cells containing a specific regulator of Ii expression. Such cells are useful, for example, in the display of autodeterminant peptides in association with MHC class II proteins. Compositions of the invention find application in methods for treating diseases, for example malignancies and autoimmune disorders, in a patient by enhancing immunological attack on undesired cells. An additional application is the isolation of autodeterminant peptides from a cell.
CN101485681B Medicament for treating burn and scald, and preparation method thereof The invention discloses a burn and scald medicine and a preparation method thereof. 100 to 150 portions of calcium oxide prepared from the following components in portion by weight and 400 to 1,500 portions of water are prepared into an aqueous solution, the aqueous solution is stirred, precipitated, clarified and deslagged, and a clear water layer of the aqueous solution is added with borneol which accounts for 0.05 to 0.1 percent of the weight of the aqueous solution and fully stirred and mixed to obtain the medicine. The medicine has the advantages of simple, convenient and quick treatmentand use, easily obtained raw materials, short treatment time, quick wound healing, and low treatment cost, and is particularly popular in broad rural patients.
US7317038 1,3-Diacetyl-8-hydroxy-2-(7-hydroxychromanon-3-yl)-9H-xanthen-9-ones; obtained from a culture of the Penicillium strain SPF-3059; prevents growth cone collapse To provide a semaphorin inhibitor; a peripheral or central nerve regeneration promoter which contains said semaphorin inhibitor as an active ingredient; and a preventive or remedy for a neuropathic disease and a neurodegenerative disease containing said nerve regeneration promoter, or the like. A low-molecular weight compound, which acts at a concentration of 10 μg/ml or below to inhibit the growth cone collapse activity of semaphorin such as semaphorin 3A, semaphorin 6C or the like and/or the nerve outgrowth inhibitory activity of semaphorin in a collagen gel and which does not substantially affect cell proliferation, is obtained from the culture of strain SPF-3059 belonging to the genus Penicillium. The low-molecular weight compound with the semaphorin inhibitory activity thus obtained exhibits the in vivo nerve-regeneration promoting action.
CN101531570B 1,2-substituted-5-acetylenyl-(or 10,11-dihydro)-5H-diphenyl[a,d] suberne (alkyl)-5-alcohol, synthesizing method and application The invention relates to a 1,2-substituted-5-acetylenyl-(or 10,11-dihydro)-5H-diphenyl[a,d] suberne (alkyl)-5-alcohol (2) compound, a preparation method and an application in a medicine for cell procedural necrosis resistance. The compound has the structure formula as the above, wherein R1 and R2 are the same or different groups and are not hydrogen simultaneously; the R1 and the R2 are selected from hydrogen, linear chain alkyl of C1-4, alkoxyl of C1-4, halogen, alkanoyl or nitryl of C1-4; and x represents a single bond or a double bond.
WO2007039592A1 Polyunsaturated fatty acids as bace inhibitors Use of polyunsaturated fatty acids of formula (I), for preventing or treating BACE mediated neurodegenerative diseases or conditions, specially Alzheimer's Disease, and pharmaceutical compositions comprising polyunsaturated fatty acids of formula (I).
US7172778 isomers of reduced folate selected from (6S)-tetrahydrofolic acid, 5-methyl-(6S)-tetrahydrofolic acid, 5-formyl-(6S)-tetrahydrofolic acid, 10-formyl-(6R)-tetrahydrofolic acid, 5,10-methylene-(6R)-tetrahydrofolic acid, 5,10-methenyl-(6R)-tetrahydrofolic acid; vitamin B6; birth defect prevention A composition for human or animal consumption for supplying folate which includes a natural isomer of reduced folate, such as (6S)-tetrahydrofolic acid, 5-methyl-(6S)-tetrahydrofolic acid, 5-formyl-(6S)-tetrahydrofolic acid, 10-formyl-(6R)-tetrahydrofolic acid, 5,10-methylene-(6R)-tetrahydrofolic acid, 5,10-methenyl-(6R)-tetrahydrofolic acid, 5-formimino-(6S)-tetrahydrofolic acid, and their polyglutamyl derivatives is disclosed. Such compositions include multivitamin preparations (with or without minerals and other nutrients); breakfast foods such as prepared cereals, toaster pastries and breakfast bars; infant formulas; dietary supplements and complete diet and weight-loss formulas and bars; animal feed (for example pet foods) and animal feed supplements (such as for poultry feed). The amount of the natural isomer of a reduced folate in a composition for human consumption can range between about 5% and about 200% of the daily requirement for folic acid per serving or dose.
WO2007082470A1 Pyrrolo-pyridazine derivatives,their preparation methods and uses The present application discloses pyrrolo-pyridazine derivatives of formula (I), (II), (III), their preparation methods, pharmaceutical compositions containing the same and their uses of acting as therapeutic agents especially tyrosine kinase inhibitors. The definitions of substituents of formula (I)-(III) are the same as description.
CN1875959A An anticancer pharmaceutical composition The invention relates the anti-cancer drugs. The drugs comprise medicinal findings and DNA duplicate inhibiting agent. The DNA duplicate inhibiting agent, from polymeric (ADP- ribose) polymerization inhibitor and DNA-dependence protease inhibitor, destructs the DNA refinishing function in tumor cell, and reduces the survivability. The medicinal findings comprises degradable absorbing high molecular polymer, and at the course of degrading and absorbing, the findings can release the DNA duplicate inhibiting agent into the tumor parts, reducing the toxicity reaction and keeping effective drug concentration. The anti-cancer drugs also comprise nitrosourea drugs, which can reduce toxicity reaction and improve therapeutic efficacy.
US20080182821 Anti-Inflammatory and/or Analgesic Composition For the Intestine Comprising Branched Maltodextrins The invention concerns a fiber-enriched anti-inflammatory and/or analgesic composition for the intestine, characterized in that it comprises branched maltodextrins having between 15 and 35% of glucoside bonds, 1 to 6, a reducing sugar content less than 20%, a polymolecularity index less than 5 and a number molecular weight Mn not more than 4500 g/mole.
CN101390867A Compositions and methods for the treatment of infection The present invention provides a combination containing at least one of the triterpene indican or analog thereof, metabolite, precursor, derivant, medicine active salt or prodrug, and an application for preparing medicament for the treatment and/or prophylaxis of viral infection. The invention also provides an application of a combined combination of the above combination and a combination containing fluvastatin or analog thereof, metabolite, derivant, medicine active salt, precursor or prodrug, for the preparation of medicament for the treatment and/or prophylaxis of viral infection. The combination and the method of the invention is further used for the prophylaxis of curee infection, and the paroxysm and development of other diseases relevant to abicin type hepatitis virus infection, such as cirrhosis, uncomp liver disease and/or hepatocelluar carcinoma.
WO2008109614A1 9-chloro noscapine and its use in treating cancers, including drug-resistant cancers 9-Chloro-nos, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-chloro-nos, and methods of preparation and use thereof are disclosed. 9-Chloro-nos is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-Chloro-nos can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL- positive cells. Thus, 9-chloro-nos is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.
CA2538910A1 Use of known active ingredients as radical scavengers The invention relates to the use of certain proton pump inhibitors in the treatment of pathological manifestations induced or influenced by free radicals.
WO2014147581A1 Plant extracts of ptaeroxylon obliquum and compounds having antimicrobial and antihelminthic activity This invention relates to an antimicrobial and antihelminthic agent comprising a compound of formula (I), to a process for extracting the antimicrobial and/or antihelminthic agent from plant material, to a composition containing the antimicrobial and/or antihelminthic agent, and to a plant extract containing the antimicrobial and/or antihelminthic agent.
US20120325209 Method for treating early severe diffuse acute respiratory distress syndrome A method for treatment of severe diffuse acute respiratory distress syndrome in an intubated-ventilated patient which includes sedating said patient with at least one alpha-2 agonist, maintaining spontaneous ventilation and applying pressure support ventilation of at least 5-10 cmH2O combined to a high positive end expiratory pressure (PEEP) of 10-24 cmH2O. A pharmaceutical composition containing at least one alpha-2 agonist suitable for treatment of ARDS in combination with, if appropriate, at least one sedative agent which does not depress ventilatory drive is also disclosed.
CN101012236A 3,7,10-trimethyl-r-aminopropyl silatranes derivative and preparing method thereof The invention discloses a synthetic 3, 7, 10-trimethyl-gamma-aminoprop-azasilicon tricyclic derivant, which can prepare pesticide, insecticide, plant growing adjuster, immune adjuster, antineoplastic drug and antibiotic drug.
EP2702991A1 A composition of entacopone A composition of entacapone comprising entacapone or pharmaceutically acceptable salts, PVPK30 and SDS is disclosed in the present invention, wherein the mass ratio of entacapone : PVPK30 : SDS is 1:0.05~0.6:0.06~0.1. The present invention also discloses preparative method and use of the composition of entacapone.
WO2011149012A1 Prophylactic or therapeutic agent for retinal/choroidal denaturation diseases comprising isoquinolinesulfonyl derivative as active ingredient, prophylactic or therapeutic method for retinal/choroidal denaturation diseases, and isoquinolinesulfonyl derivative or pharmaceutically acceptable salt thereof and use thereof A compound represented by general formula (1) or a salt thereof has an inhibitory effect on photoreceptor cell death and/or visual cell death in a light-induced damage mouse model, and is therefore useful as a prophylactic or therapeutic agent for retinal/choroidal denaturation diseases that do not substantially involve neovascularization (e.g., atrophic age-related macular degeneration, retinitis pigmentosa, gyrate atrophy of choroid and retina) and retinal and choroidal disorders associated with the aforementioned diseases.
WO2007009911A1 PYRIDO [2 , 3-D] PYRIMIDINE-2 , 4-DIAMINE COMPOUNDS AS PTPlB INHIBITORS The present invention is concerned with compounds of formula (I) wherein R1, R2, R3, R4 and X are as described in the description and claims. The compounds are inhibitors of PTP1B. Accordingly, the compounds can be used for treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.
CN1927166A Terazosin slowly releasing preparation This invention involves a terazosin sustained-release preparation. Taking hypromellose, polypropylene resins, carbopol category, soluble / insoluble salts of alginic acid, beeswax, carnauba wax, stearic acid alcohol, stearic acid, polyethylene glycol, polyethylene glycol mono-ester stereo-oate and one of other excipients which have the function of slow-releasing or the combination of a few as the slow-releasing material, and it can be rapidly and effectively treat the diseases of hyperplasia of prostate gland and hypertension.
US20110092557 Neuraminidase Inhibitors And Compositions And Methods Related Thereto The present invention provides compounds comprising amino acid R groups, compositions comprising the same, and methods of inhibiting neuraminidase and/or treating influenza, Pseudomonas aeruginosa, or Bacteroides fragilis infection in a mammal.
WO2013189241A1 Pyrimidine diamine derivative, preparation method therefor, and pharmaceutical uses thereof A pyrimidine diamine derivative as represented by formula (I), pharmaceutical salts thereof, pharmaceutical compositions containing the derivative, a preparation method therefor, and pharmaceutical uses thereof. The compound and the pharmaceutical salts thereof or the pharmaceutical composition containing the compound can be used for preparing Syk protease inhibitors.
CN101254186A Medicament use of myricetin The invention discloses a new medical use of myricetin, belonging to the technology field of medicines. Through acetic acid writhing test, formaldehyde-induced pain test, glacial acetic acid-induced capillary permeability test, dimethybenzene-induced mouse ear swelling test, egg white and carrageenin-induced paw edema test, test of leukocytoplania of pleurisy caused by carboxymethyl cellulose, granuloma (chronic) inflammation test, and screening of adjuvant arthritis animal models with primary and secondary inflammations, the myricetin is found to have high antiphlogistic and analgesic activity and can prevent and treat adjuvant arthritis, the antiphlogistic activity of myricetin is equivalent to that of aspirin but no gastrointestinal toxicity, and the anti-rheumatoid arthritis activity of myricetin is equivalent to that of Tripterygium wilfordii, and the myricetin has liver protecting effect and is an ideal drug for preventing and treating acute and chronic inflammations and rheumatoid arthritis. The myricetin can be prepared into various preparations with pharmaceutically-acceptable carrier for relieving inflammations, reliving pain and treating rheumatoid arthritis.
US7601730 Carboxylic acid derivatives, their preparation and use Carboxylic acid derivatives where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
US20100130469 2, 6-naphthridine derivatives The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof.
WO2005025557A1 An agent for plasminogen-activation and matrix metalloproteinase associated conditions and methods of use The present invention provides methods and compounds useful in the treatment of conditions such as metastatic cancer spread and atherosclerosis using oxamflatin and derivatives thereof. It has been found that oxamflatin and derivatives thereof are able to modulate the plasminogen-activation/matrix metalloproteinase system leading to the ability to control degradation of extracellular matrix proteins.
WO2013081452A1 Phosphatidylinositol The invention relates to a new pharmaceutical compound, diacyl phosphatdylinositol in which both the sn-1 and the sn-2 place are taken by stearic acid (18:0) (diacyl [18:0; 18:0] phosphatidylinositol), more preferably, wherein said diacyl phosphatidylinositol is compound 1 as depicted in Fig. 10 or a racemate of compounds 1 and 2 as depicted in Fig. 10. Said pharmaceutical compound and pharmaceutical compositions comprising this compound are specifically useful for the treatment of a disease or a condition wherein suppression of T-cell activation is desirable, such as asthma, diabetes Type 1, rheumatoid arthritis, inflammatory bowel disease or psoriasis. Also part of the invention are food items containing the compound(s) of the invention and use thereof in a diet to treat or prevent the disease or condition mentioned above
US20110281957 Enhanced bioactive formulations of resveratrol Methods and formulations for increasing the water solubility and/or bioavailability of resveratrol are disclosed. The formulations may be employed to treat a disease states, including cancer.
WO2010151638A1 Jnk inhibitors for use in treating spinal muscular atrophy The brain specific isoform (JNK3) of c-Jun NH2-terminal kinase (JNK) has been found to mediate the degeneration of spinal motor neurons caused by SMN deficiency in spinal muscular atrophy (SMA). Moreover, the ability of JNK inhibitors to reduce degeneration of neurons lacking SMN is also disclosed. The JNK signaling pathway can therefore mediate neurodegeneration in SMA and represents a therapeutic target for treatment of SMA.
CN102988324A Preparation for glipizide compression-coated controlled-release tablets The invention provides a glipizide compression-coated controlled-release tablet preparation which is in the form of zero-order release for a long time, and the preparation is tablets prepared by a compression-coating technology. An indissolvable medicine, namely, glipizide, is solubilized by adopting an inclusion compound technology, and the integrated tablets are formed by pressing tablet cores and shell layers, wherein both of the tablet cores and the shell layers contain glipizide and gel-forming macromolecular substances, and disintegration-inhibiting substances capable of enhancing gel toughness are further contained in the shell layers. The glipizide compression-coated controlled-release tablets according to the invention can release medicines with a constant speed or an approximately constant speed in 24 hours in vitro and in vivo, has the characteristics of being low in cost, easy to realize mass production and the like compared with the conventional osmotic pump-type controlled-release tablet preparations on the market, and can provide a research basis and a production technology platform for the development of controlled-release preparations. The glipizide compression-coated controlled-release tablets only need to be taken once everyday, thus enhancing clinical compliance.
US20090123530 Liposome Drug Delivery This invention comprises pharmaceutical compositions for administering a biologically active compound to an animal. Particularly provided are proliposomal compositions that are advantageously used to deliver biologically active compounds to the gastrointestinal tract after oral administration.
US20120220660 Composition With Preventive or Improvement Effect on Symptoms or Diseases Associated with Stress-Induced Behavior Disorders A composition with a preventive or improvement effect on symptoms or diseases associated with stress-induced behavior disorders, comprising arachidonic acid and/or a compound comprising arachidonic acid as a constituent fatty acid.
US20070287742 Subsitituted Gamma Lactams As Therapeutic Agents A compound comprising or a pharmaceutically acceptable salt, prodrug, or a metabolite thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.
WO2014018570A1 Cystathionine-υ-lyase (cse) inhibitors Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit cystathionine -γ-lyase (CSE). Also described herein are methods for using such CSE inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from CSE inhibition.
US20130164259 1,4-substituted piperazine derivatives and methods of use thereof The present invention relates to 1,4-Substituted Piperazine Derivatives, compositions comprising one or more 1,4-Substituted Piperazine Derivatives, and methods of using the 1,4-Substituted Piperazine Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
EP2506873A2 Vaccine against neoplastic or cancerous lesions caused by human papillomavirus (hpv), procedures, uses and methods Vaccine against neoplastic or cancerous lesions caused by human papillomavirus (HPV), which comprises E7 peptide spherical particles and, as an option, an adjuvant, where spherical particles may be oligomeric. The oligomeric spherical particles may have a diameter in the vicinity of 50 nm and a molecular weight in the vicinity of 700 kDa. The vaccine may be helpful to prevent or treat human papillomavirus (HPV)-related lesions or do both things at the same time.
EP2014303A2 APO-2L receptor agonist and CPT-11 synergism Methods of using effective amounts of Apo-2L receptor agonists and CPT-11 to induce apoptosis and suppress growth of cancer cells are provided.
US20080031965 Oral Preparations and Process for Production Thereof Disclosed herein are oral preparations and their production process. The oral preparations are each composed of a complex and a coating composition applied on the complex. The complex has been obtained by dispersing or dissolving a drug having an unpleasant taste and a gastric high-molecular compound in a low melting-point substance heated to and molten at its melting point or higher and granulating the resulting mixture. The coating composition is composed of an insoluble high-molecular compound and a disintegrator at a weight ratio of from 80:20 to 99:1. In the form of microparticles or the like that contain the drug having the unpleasant taste, each oral preparation according to the present invention can maintain the masking of the unpleasant taste of the drug and the release profile of the drug even under acidic conditions.
WO2008012010A1 Fused oxazoles & thiazoles as histamine h3- receptor ligands The present invention relates to compounds comprising fused oxazole or thiazole derivatives of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, wherein A is a cyclic amine which is linked to the propylene group via an amino nitrogen; B is selected from the group consisting of heteroaryl, 5-8-membered heterocycloalkyl, 5-8-membered cycloalkyl; X is either N or CH; Y is either O or S.
US7560486 An isotonic lipid emulsion free of vegetable oils:(i) 78 to 95% by weight of medium chain triglycerides (MCT), (ii) 5 to 22% by weight of fish oil; to increase the amount of omega-3 fatty acids of cell membranes of organs and tissues The present invention relates to a composition and method for rapidly modifying the fatty acid composition of cell membranes of organs and tissues, in particular to increase the amount of omega-3 fatty acids of cell membranes of organs and tissues by parenterally administering to the human or animal body a supply of fatty acids in the form of an isotonic lipid emulsion comprising fatty acid triglycerides.
WO2014026161A1 Vitamin supplement compositions for injection The embodiments relate to improved vitamin supplement compositions formulated for administration to patients, particularly improved vitamin compositions formulated for use in cosmetic or therapeutic applications. The compositions may be used to slow aging process and promote wellness including treating a vitamin deficiency, skin conditions, improving skin appearance, wound healing and scar prevention and hair loss.
US20100093781 Imidazo [1, 2-a] pyrrolo [3, 2-c] pyridine compounds useful as pestivirus inhibitors The present invention relates to a series of novel imidazo[1,2-α]pyrrolo[3,2-c]pyridines (or also named 6H-1,3a,6-Tri-aza-αy-indacenes) and derivatives thereof, according to formula: (I); The present invention also relates to processes for the preparation of imidazo[1,2-α]pyrrolo[3,2-c]pyridines, their use as. a, medicine, their use to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with viruses belonging to the family of the Flaviviridae and more preferably infections with Bovine Viral Diarrhea virus (BVDV).
CN103006653A Applications of 2,4-disubstituted thiazoles derivatives being taken as DHODH (dihydroorotate dehydrogenase) inhibitor The invention relates to applications of a 2,4-disubstituted thiazoles compound in pharmaceutical chemistry and pharmacotherapy. Specifically, the invention relates to applications of a compound shown in formula I (described in the specification) and a medicinal composition of the compound in preparation of medicines used for treating diseases related to DHODH (dihydroorotate dehydrogenase).
CN103356532A Application of Sarcaboside B in medicine used for treating breast cancer The invention discloses an application of Sarcaboside B in preparation of a medicine used for treating breast cancer and belongs to the technical field of new applications of medicines. In vitro MTT (methyl thiazolyl tetrazolium) antineoplastic activity evaluation shows that Sarcaboside B has an obvious inhibitory effect on growth of human breast cancer cell strains 4T1, MCF-7, MDA-MB-231 and MCF-7B, so that Sarcaboside B can be used for preparing an anti-breast-cancer medicine and has a good development application prospect; the application of Sarcaboside B in preparation of the medicine used for treating breast cancer is disclosed for the first time, a brand new skeleton type is adopted, and Sarcaboside B has an unexpected inhibitory activity on breast cancer cells.
US20110300225 Nutritional compositions with coated lipid globules The present invention relates to a nutritional composition for infants and/or toddlers comprising a lipid component which has a lipid globules coated with phospholipids. The composition is used for increasing bone mineral content, bone mineral density, preventing osteoporosis, and/or preventing ostopenia.
WO2014015235A2 3,5,n-trihydroxy-alkanamide and derivatives: method for making same and use thereof The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.
US6926178 Valve with a two-component seal A valve for an aerosol container including a valve body, a valve stem having a dispensing passage, and a sealing ring contacting the valve stem. The valve stem is slidably moveable relative to the sealing ring from a valve-closed position to a valve-open position in which the interior of the valve body is in communication with the dispensing passage. The sealing ring includes a flexible component and a rigid component. The valve is preferably a metering valve.
CN101890128A Sore washing wine The invention discloses a manufacturing method of a sore washing wine, which is realized by the following technical scheme: placing white mulberry root-bark, hay and rice grass into a nasonry for baking burned black, evenly mixing with lime to be packed in a cloth bag, placing the cloth bag into a wine tank, soaking for 24 hours, heating for 20-30 minutes, then keeping the tank sealed for 10 days, and taking out to obtain the finished wine. The sores can be healed after being washed for three times by utilizing the sore washing wine prepared by the method.
US20120232045 Methods and systems for prognosis of a patient's response to treatment of androgenetic skin disorders Methods and systems are described for prediction of a patient's response to a drug for treating androgenetic skin disorders such as alopecia, acne, and hirsutism. For a given drug such as anti-androgens and 5-alpha-reductase inhibitors, and a given dosage, the likely responsiveness of that drug and dosage may be determined, for example, by generating a set of patient scores based on a patient profile, including genetic sample information, and comparing that scores to a set of reference information.
CN101244071A Method for preparing sodium fructose diphosphate injection The invention relates to a preparation method of fructose sodium diphosphate injection, belonging to the technical field of medicine. The preparation method is: medical solution is treated by cation exchange resin, which can reduce acidity, remove metal cation, absorb colorful impurities and pyrogens, increase the clarity of the medical solution, avoid the defects of decreasing the product purity, increase osmotic pressure, and influencing medication safety caused by acid radical ion when acid is used to regulate acidity, and provides a stable fructose sodium diphosphate injection with high purity. The fructose sodium diphosphate injection is applied to intravenous injection or intravenous drip in clinical practice, and is suitable for low phosphorus acidemia. The preparation method has the advantages: the preparation method is simple and controllable, and the prepared product quality is stable and safe for clinical use.
US20110312951 C-Ring Modified Tricyclic Benzonaphthiridinone Protein Kinase Inhibitors and Use Thereof Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.
US7060725 Substituted sulfamate anticonvulsant derivatives The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.
US20060263373 Utilization of an aminopeptidase inhibitor The invention concerns the utilization of at least one aminopeptidase inhibitor for the production of a medicament used in the treatment of tumor diseases and/or immune diseases, whereby the at least one aminopeptidase inhibitor causes blocking of polarization of invasive human or animal tumor and/or immune cells by modifying at least one surface protein CD13 as member of a protein network on the surface of the tumor and/or immune cells, whereby the protein network comprises up to 30 surface proteins from a defined group. The invention also concerns a pharmaceutical preparation and a method for identifying at least one additional inhibitor acting in combination with the at least one aminopeptidase inhibitor.
WO2008075993A1 The use of diethylamine as analgesic in pharmaceutical preparations The present invention refers to the use of diethylamine as analgesic in pharmaceutical preparations, for the treatment of any kind of pain. The present invention refers to diethylamine used as analgesic in the treatment of any kind of pain in doses between 10 mg and 1g, and also to the use of diethylamine as active substance for the preparation of analgesic drugs.
CN101023985A Medicine for treating tinea mannum and tinea pedis and preparing method thereof The present invention relates to a medicine for effectively curing tinea manuum and tinea pedis. Said medicine is made up by using (by weight portion) 25-35 portions of scutellaria root, 25-35 portions of flavescent sophora root, 1200-1800 portions of edible vinegar, 25-35 portions of edible salt, 50-70 portions of alum, 8-12 portions of aspirin and 15-25 portions of phenol through a certain preparation process. Said invention also provides the concrete steps of said preparation process.
CN102633777A Dabigatran etexilate 2-ketoglutarate as well as preparation method and application thereof The invention provides dabigatran etexilate 2-ketoglutarate shown in a general formula (I), hydrate and/or a solvate thereof. In the formula (I), n is 1, 2 or 3. The invention also provides a preparation method of dabigatran etexilate 2-ketoglutarate as well as hydrate and/or the solvate thereof and application in preparation of medicaments for treating or preventing cardiovascular diseases.
CN103319456A Dihydropyridine compounds, and compositions, preparation methods and applications thereof Dihydropyridine compounds are disclosed, and are compounds represented by the following general formula (I), wherein R1 is selected from alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 is selected from hydrogen, alkyl, substituted alkyl or a heterocycle formed by R2 and R3; and R3 is selected from alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, or a heterocycle formed by R3 and R2. The invention also discloses preparation methods for the compounds represented by the general formula (I), and pharmaceutical compositions and applications of the compounds.
CN101537005B Codein and chlorphenamine compound sustained release capsules The invention discloses codein and chlorphenamine compound sustained release capsules. The sustained release granules are made from the following raw materials by weight: 10-11.1 parts of codein, 2-2.2 parts of chlorphenamine, 1-2 parts of a lubricant, 18.9-86 parts of a sustained release matrix material and 0-12.4 parts of a filling agent. The sustained release matrix material is two or three ofhydroxypropyl emthylcellulose, acrylic resin and ethyl cellulose, wherein, the acrylic resin and the ethyl cellulose totally accounts for 10.9-31.5%. The capsules are obtained by the following steps:evenly mixing the codein, the chlorphenamine and the sustained release matrix material; adding a binder to prepare a soft material and sieving with a 6-24-mesh sieve; preparing damp granules, drying and granulating; and adding the lubricant, evenly mixing and then encapsulating to obtain the finished product.
US20080044406 Neuroactive fragments of APP The application provides novel neuroactive fragments of human amyloid precursor protein (APP). The fragments include sequence from the Aβ region of APP but also extend upstream. The fragments are soluble in aqueous solution most bands are about 10 kDa and above and do not correspond with the expected molecular weight of a dimer or trimer. The fragments and subfragments thereof can be used as immunogens in methods of immunotherapy to treat Alzheimer's and other amyloidogenic diseases characterized by deposits of Aβ in the brain. Antibodies to the part of the fragment upstream from APP or the interface between Aβ and the upstream sequence can also be used in such therapeutic method. The fragments are also useful as markers, which can be detected for diagnosis or prognosis of disease or for screening agents.
WO2014096418A3 Micrornas as therapeutics and biomarkers for epilepsy The present invention relates to a pharmaceutical composition for use in the treatment or prevention of epilepsy, comprising a means for alleviating or reversing the effect of a dysregulation of a miRNA molecule. The invention further relates to a vaccine for use in the treatment or prevention of epilepsy, to a biomarker or group of biomarkers associated with epilepsy, a composition for diagnosing, detecting, graduating, monitoring or prognosticating epilepsy or a predisposition for epilepsy, a method or assay for diagnosing, detecting, graduating, monitoring or prognosticating epilepsy or a predisposition for epilepsy. Also envisaged is a method for monitoring epilepsy therapy, a method of identifying an individual eligible for an epilepsy therapy, a corresponding diagnostic kit and the use of a biomarker or a group of biomarkers for diagnosing, detecting, graduating, monitoring or prognosticating epilepsy or for identifying pharmaceutically active agents useful in the treatment or prevention of epilepsy.
WO2008061409A1 Enteric coated formulation comprising alkaline active agent and its preparation process An oral enteric coated formulation comprises alkaline pH regulator as active agent and its preparation process, said alkaline agent is selected from: sodium bicarbonate, potassium bicarbonate, sodium carbonate, citric acid, sodium citrate, potassium citrate, potassium hydrogen citrate, potassium-sodium hydrogen citrate, and mixtures thereof.
CN103638011A Application of Artoxanthochromane to monoamine oxidase (MAO) inhibitor The invention provides application of Artoxanthochromane to a monoamine oxidase (MAO) inhibitor. Compared with an existing MAO inhibitor, the MAO inhibitor has the advantage that the inhibition activity and the selectivity to MAO-A and MAO-B are greatly improved. The application of the Artoxanthochromane to the monoamine oxidase (MAO) inhibitor is firstly disclosed, is high in MAO inhibition activity, has remarkable substantive distinguishing features, and has a remarkable progress in treatment of diseases related to MAO imbalance.
US20120129944 Stabilized composition comprising at least one adrenergic compound A stabilised composition comprising at least one adrenergic compound and at least one antioxidant selected from the group consisting of a bisulfite, a metabisulfite and a sulfite compound.
CN102617585A Furocoumarin derivative, preparation method thereof and use thereof The invention which belongs to the pharmacological field relates to a heterocyclic compound treating furocoumarin as a mother nucleus and having a structural formula represented by formula I, a preparation method thereof, and a use of the compound in the preparation of medicines for treating the gout disease.
CA2623858A1 Stabilized chlorine dioxide and hypochlorous acid in a liquid biocide A liquid biocide containing stabilized chlorine dioxide and hypochlorous acid for various uses, including use as a teat dip or dairy animals. The stable, prophylactic biocide consists essentially of 0.10-20.0% by weight of a chlorite salt, 0.1--3.0% by weight of an acid, 0.10-2.0% by weight of an alkaline agent, and the balance water. Chlorite salt reacts with the acid to form germicidal chlorine dioxide and hypochlorous acid. The acid constituency and the alkaline agent constituency regulate the pH of the solution such that the biocide is stable when mixed for a period greater than two months. The present disclosure also includes a method of producing a stable, prophylactic biocide for dairy cattle, the method comprising 0.10-20.0% by weight of a chlorite salt, 0.10-3.0% by weight of an acid, 0.10-2.0% by weight of an alkaline agent, and the balance water in a container, and sealing the container. In the method, the acid and alkaline agent constituencies regulate the pH of the solution such that the formation of hydronium ions from the acid is correspondingly regulated to stabilize the solution for a period greater than two months from the date of sealing.
CN101624413B Chalcomycin compounds and preparation and application of same The invention relates to chalcomycin compounds and the preparation and the application of the same, belonging to the medical technology field. The chalcomycin compounds of formula 1, formula 2 and formula 3 are prepared in such a way that marine streptomyces M491 is fermented to accumulate crude extract, and the crude extract is separated with various chromatographies such as the silica gel chromatography. The chalcomycin compounds of the formula 1, the formula 2 and the formula 3 can be used for preparing antineoplastic, antibacterial or antiviral medicament. The chalcomycin compounds with novel chemical structures are searched by utilizing marine microbial resources, and the chalcomycin compounds have antitumor activity, can inhibit various human tumor cells and are novel medicaments orleading compounds in the clinical field.
US7652061 (R)-1-{2-[3-(5-Methyl-2-pheny-oxazol-4-ylmethoxy)-phenyl]-acetyl}-pyrrolidine-2-carboxylic acid; dyslipidemia, hyperlipidemia, hypercholesteremia, or type-2 diabetes Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis, Crohn's disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.
US20110003835 Methods for the treatment of respiratory depression This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stoke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning, hi a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.
CN102225050A Method for preparing famotidine sodium chloride injection by inclusion method and product prepared by using the same The invention relates to a method for preparing a famotidine sodium chloride injection by an inclusion method and a product prepared by using the same. The method is characterized in that sulfobutyl ether-beta-cyclodextrin is used as an including agent of famotidine, and famotidine is firstly dissolved in glacial acetic acid and then added into a sulfobutyl ether-beta-cyclodextrin saturated solution to allow sulfobutyl ether-beta-cyclodextrin to include famotidine, and the sulfobutyl ether-beta-cyclodextrin including famotidine is dissolved in water; the weight part ratio of famotidine to sulfobutyl ether-beta-cyclodextrin is (1:5)-(1:10); the quantity of glacial acetic acid is 5-7 times of that of famotidine based on weight part; and excessive sterilization at 121 DEG C for 15 minutes is adopted. The method provided by the invention has the following advantages: related substances are controlled within 2%, which is far lower than 5% of domestic like-products, and the sterilization is changed from a residual probability method to an excessive sterilization method, which ensures 100% sterilization, greatly improves product quality and enhances the safety of medicine in clinical applications.
US7727965 C-glycosylisoflavones having alkylaminoalkoxyl substituent, preparation and use of the same The present invention relates to C-Glycosylisoflavones having alkylaminoalkoxyl substituent and pharmaceutically acceptable salts thereof, a process for the preparation thereof, pharmaceutical compositions comprising an effective amount of a compound of the formula (I), and to the use of these compounds or compositions for the treatment or prevention of cardio- and cerebrovascular diseases, in particular for the treatment of various cardiocerebral hypoxic-ischemic diseases, for the treatment or prevention of diabetes mellitus and complications thereof, and for the treatment or prevention of chemical poisoning, in particular alcoholism.
CN102370640A Compound amino acid preparation for hemodialysis and hemodialysis preparation containing same The invention relates to a compound amino acid preparation for hemodialysis and a hemodialysis preparation containing the same. The invention provides a preparation for modulating disorder of plasma aminogram of hemodialysis patients by using a plurality of essential amino acids and semi-essential amino acids, specifically relates to a solid powder form or liquid bicarbonate hemodialysis preparation used for treating nephrosis and containing compound amino acids, and especially to a hemodialysis preparation containing L-leucine, L-isoleucine, L-valine, L-threonine, L-phenylalanine, L-methionine, L-tryptophan, L-lysine, L-histidine, L-arginine and a pH conditioning agent (e.g., acetic acid, citric acid, malic acid, lactic acid and hydrochloric acid) and a preparation method thereof. The hemodialysis preparation further contains sodium chloride, potassium chloride, calcium chloride, magnesium chloride and sodium bicarbonate, and can also include glucose. Compared to conventional bicarbonate hemodialysis preparations, the preparation provided in the invention has the advantages of partly modulating disorder of plasma aminogram of hemodialysis patients and reducing side effects in hemodialysis treatment.
US20080166408 Oral Dosage Form Comprising Rosiglitazone An oral dosage form, such as a bilayer tablet, comprising a first layer of a first composition and a second layer of a second composition, each composition comprising 5-[4-[2-(N-methyl-N-(2 pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione or a pharmaceutically acceptable salt or solvate thereof, (‘the drug’) and a pharmaceutically acceptable carrier therefor, wherein the first and second compositions are arranged to release drug at differing release rates on administration; a process for preparing such a dosage form; and the use of such a dosage form in medicine.
WO2010139982A1 Indole derivatives for the stimulation of stem cell proliferation The present invention relates to indole derivatives of formula (I) and Formula (II) which possess potent antiprion activity and stem cell proliferative properties. The invention also relates to the use of such compounds to treat prion-related diseases and in stem cell therapies.
CN102125569A Application of 1, 6-bisphosphate fructose in preparation of anti-cancer medicaments The invention provides application of 1, 6-bisphosphate fructose and medicinal salt thereof in the preparation of medicaments for treating and preventing tumors. The tumors comprise digestive system tumors, brain tumors, sarcoma, leukemia, lung cancers, and male tumors (prostatic cancers) and female tumors (breast cancers). The 1, 6 bisphosphate fructose provided by the invention has low toxicity and high safety, has certain degree of cell toxicity to humanized and tumor cells and is especially sensitive to bowel cancers and glioma after being confirmed in in-vitro experiments, and the activity is further improved after the 1, 6-bisphosphate fructose is used in combination with other energy metabolism related anti-tumor medicaments. Thus, the medicaments prepared from the 1, 6-bisphosphate fructose are suitable for treating acute tumors and preventing the postoperative recurrence of the cancers of cancer patients. The structural formula of the 1, 6-bisphosphate fructose is shown in the specification.
CN1965863A Method for preparing compound amino acid oral liquid by using animals placenta The invention relates to a method for using animal placenta composite amino acid oral agent, wherein its production comprises that: animal placenta pretreatment, acid treatment, acid removing, dispersing, cracking, anti-effusion separation, shaping, emulsifying, and packing. The invention uses pig and sheep placentas. It can reduce cost and improve yield, to produce 18 kinds of protein amino acid and one non-protein amino acid mixture, which contain 6 kinds of needed amino acids. The amino acid content can reach 3.95mg/ml, and the needed amino acid content reaches 0.76mg/ml. The production can kill virus and enzyme, and separate heavy metal ion.
US7208602 N-sulfonyl- azetidines, pyrrolidines, piperidines and hexamethylenimines; treatment and prevention of Alzheimer's Disease and other diseases relating to the deposition of amyloid protein. This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
CN102512677A Application of guanylate cyclase inhibitor to preparation of medicament for inhibiting myopia The invention relates to a preparation method of a medicament for delaying and inhibiting myopia, in particular to the application of a guanylate cyclase inhibitor for the preparation of a medicament for inhibiting myopia. The guanylate cyclase inhibitor serves as the myopia-inhibiting medicament to reduce the content of cGMP (guanosine-3',5'-cyclized-phosphate, cyclic guanosine monophosphate) and then, can inhibit the formation of animal experimental myopia.
EP2036909A1 Quaternary ammonium salt compounds of spirocyclopiperazines, preparation methods and uses thereof Compounds represented by general formula (I), their stereoisomers, tautomers, derivatives, prodrugs or pharmaceutically acceptable salts, and their preparation methods or uses for the manufacture of a medicament of analgesics. In which R1 is selected from H, substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; A is bond, or saturated or unsaturated straight-chain or branched-chain hydrocarbon radical; R2, R3 are each independently hydrogen or methyl, which linked with any position of spirocyclo-structure; n and m are each independently integer between 0-2, do not represent 0 at the same time; B and D are each independently C1-C3 straight-chain or branched-chain alkylene; Y is selected from -CHR4-, O, S, -S(O)-, -SO2-, -NR4- and substituted or unsubstituted phenylene, in which R4 represents H, C1-C6 saturated or unsaturated alkyl, methyl or ethyl substituted by substituted or unsubstituted aryl or heteroaryl; and X- is pharmaceutical acceptable organic or inorganic anion. These compounds can be used as muscarine receptor (M-receptor) and/or nicotine acetylcholine receptor (N-receptor) agonist or antagonist. These compounds have good analgesic effect without side effect such as addiction.
US7718645 4-[4-(4-Amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cycloalkylalkyl nitriles, carboxy acids or esters, amides, e.g., a -cyclohexylacetonitrile; diglyceride acyltransferase inhibitors for treating type II diabetes and obesity The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c, R5d, Q, A, Z, and R7 are as described herein; compositions thereof; and uses thereof.
CN1607204A Cyclophosphamide quaternary ammonium salt derivant and its synthesis and use Said invention relates to a compound and stereoisomer, tautomer, derivative, prodrug and pharmacy acceptable salts wherein R#+[1],R#+[2],R#+[3],R#+[4],R#+[5],R#+[6], m, n, q, Z and X just like defined in instruction. Said invention also refers to the preparation of said compound and use in treating tumour.
CN101669903A Preparation method of ibuprofen aminophenol injection The invention discloses a preparation method of ibuprofen aminophenol injection. After a plenty of experiment researches, the researchers finally find a way to prepare the ibuprofen aminophenol injection. The preparation method comprises the steps of making ibuprofen and aminophenol into a compound, combining with proper accessories and making into injection. By making ibuprofen and aminophenol into a compound, the invention can solve the problem of the inferior water-solubility of the ibuprofen. Making the compound into injection brings convenience to the patient who can not take orally. Theinvention has fast effect and obvious pharmacological action.
CN103349655A Tamoxifen citrate enteric capsules The invention relates to tamoxifen citrate clathrate compound enteric capsules, the preparation method of which comprises the steps of preparing tamoxifen citrates into clathrate compounds and further preparing the clathrate compounds into the enteric capsules.
EP2488530A1 Spirocyclic piperidine derivatives useful as renin inhibitors Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is -(C=O)-, -CH2- or =CH-; U is a bond or -CH2-, or, when V iS =CH-, U is-CH=; X is =CH-, =CF-, =C(OR3)-, or -(C=O)-; and Y is =CH-, =CF-, =N-, or, for the case when X is -(C=O)-, Y is -N(R3)-.
US20070286896 Therapeutic or Diagnostic Drug for Inflammatory Disease Comprising Targeting Liposome There is provided targeting drug delivery system (DDS) nanoparticles that can be accumulated in target tissues such as inflammatory sites of inflammatory diseases and can thus be utilized in a therapeutic or diagnostic DDS for locally delivering drugs or genes to the affected parts. The present invention provides a pharmaceutical composition for the medical treatment or diagnosis of an inflammatory disease comprising a sugar-modified liposome having a sugar chain bound to the membrane of the liposome.
EP2670740A1 Amidobenzothiazoles and process for the preparation thereof The present invention provides a compound of general formulae A useful as potential anti-cancer agents against human cancer cell lines and a process for the preparation thereof. Where in R, R1, R2=H, alkyl, alkoxy, halo, haloalkyl, halomethoxy, nitro and G= Where in R, R1, R2=H, alkyl, alkoxy, halo, haloalkyl, halomethoxy, nitro and G=
US20080269228 Hydrazide-containing hepatitis c serine protease inhibitors The present invention relates to novel hydrazide-containing compounds of Formula I or Formula II, including pharmaceutically acceptable salts, esters, or prodrugs thereof which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
CN101664448B Acne ointment as well as preparation method and quality detection method thereof The invention discloses an acne ointment as well as a preparation method and a quality detection method thereof. According to parts by weight, the acne ointment is made from 0.8-1.2 parts of sulfur, 0.8-1.2 parts of rhubarb, 5-7 parts of stearic acid, 1-3 parts of glyceryl monostearate, 7-11 parts of castor oil, 0.04-0.06 part of ethyl p-hydroxybenzoate, 4-6 parts of glycerol, 0.7-0.8 part of triethanolamine and 20-28 parts of water. Compared with the prior art, the acne ointment has the efficacies of clearing way heat and removing toxicity, eliminating dampness and killing insects, can prevent and treat acne comprehensively, and is characterized by convenient carrying-over and use, comfort, obvious curative effect and less toxic side effects; and the quality detection method has strong specificity, high precision and good stability, and can effectively ensure the clinical treatment efficacy of the acne ointment.
WO2009016072A3 A morpholinyl anthracycline derivative combined with protein kinase inhibitors The present invention provides the combined use of a morpholinyl anthracycline derivative of formula (I) as defined in the specification or a pharmaceutically acceptable salt thereof, such as nemorubicin hydrochloride, and a protein kinase (PK) inhibitor, in the treatment of tumors. Also provided is the use of the said combinations in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.
US20120330436 Bone graft substitute A bone graft substitute in the form of an implantable three-dimensional scaffold that includes calcium phosphate and has pores. The scaffold is impregnated with a calcium and/or phosphate containing substance, and the dissolution rate DRS of the scaffold is slower than the dissolution rate DRD of the calcium and/or phosphate containing substance.
EP1506197A1 Acyl bicyclic derivatives of pyrrol The invention relates to anti-viral agents of Formula (I); wherein: RA represents OR1, NR1R2, or R1 wherein R1 and R2 independently represent hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; RB represents C(O)R3 wherein R3 represents aryl or heteroaryl; RC represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; RD represents hydrogen and RE represents hydrogen, OR4 or SR4, or RD and RE together with the carbon atom to which they are attached form a carbonyl group or a thiocarbonyl group; when RE is hydrogen, OR4 or SR4, RG and RH are both hydrogen; when RD and RE together with the carbon atom to which they are attached form a carbonyl group or a thiocarbonyl group, RG represents hydrogen and RH represents hydrogen, OR4 or SR4, or RG and RH together with the carbon atom to which they are attached form a carbonyl group or a thiocarbonyl group; R4 represents hydrogen, C1-6alkyl or aryl; when RD and RE together with the carbon atom to which they are attached form a carbonyl group or a thiocarbonyl group, and RG and RH are both hydrogen or RG and RH together with the carbon atom to which they are attached form a carbonyl group or a thiocarbonyl group, then RF represents O, S, NR5 or CR6R7, otherwise RF represents CR6R7; R5 represents hydrogen, C1-6alkyl, arylalkyl or aryl;R6 and R7 independently represent hydrogen, C1-6alkyl, arylalkyl or heteroarylalkyl;RJ represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and enantiomers thereof;provided that when RA is OR1 then R1 is other than tert-butyl, for use in medical therapy. A process for the preparation of compounds of Formula (I) and methods of using them in HCV treatment are provided.
EP2179999A1 Fused tricyclic compound having aldose reductase inhibitory activity A fused tricyclic compound having aldose reductase inhibitory activity and shown by the following formula, wherein R1 independently represents 1 to 3 atoms or substituents selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, cycloalkyl, alkylene, or alkoxy group, and a protected or unprotected hydroxyl or carboxyl group, R2 represents a protected or unprotected carboxyl group, R3 independently represents 1 or 2 atoms or substituents selected from a hydrogen atom, a halogen atom, an oxo group, a substituted or unsubstituted alkyl or alkoxy group, and a protected or unprotected carboxyl group, A represents an alkylene group, and B represents an oxygen atom, a sulfur atom, or a group shown by the following formula, wherein R4 represents an alkyl or aryl group substituted with an aryl, cycloalkyl, or heterocyclic group, and X represents an oxygen atom or a sulfur atom.
CN101785747A Use of monosaccharides and composition The present invention relates to the use, especially the cosmetic use, of at least one monosaccharide chosen from mannose, rhamnose and a mixture thereof, for reducing or preventing the signs of ageing of the skin or its integuments. The present invention also relates to a cosmetic composition and a device containing it.
US20080279869 Method for reducing neuronal degeneration by administering cns-derived peptides or activated t cells Compositions are provided for promoting nerve regeneration or reducing or inhibiting degeneration in the CNS or PNS to ameliorate the effects of injury or disease. The composition includes an active ingredient selected from:(a) a peptide obtained by modification of a self-peptide derived from a CNS-specific antigen, which modification consists in the replacement of one or more amino acid residues of the self-peptide by different amino acid residues, such modified CNS peptide still being capable of recognizing the T-cell receptor recognized by the self-peptide but with less affinity; (b) a nucleotide sequence encoding such a peptide; (c) T cells activated by such peptide; and (d) any combination of (a)-(c). The peptide is preferably obtained by modification of the self-peptide p87-99 of MBP, more preferably, by replacing lysine 91 with glycine (G91) or alanine (A91) or by replacing proline 96 with alanine (A96).
CN1775289A Multi vitamin oral disintegrating tablet formulation and its preparing method The present invention provides a multivitamin oral disintegrant tablet prescription and its preparation method. Said prescription composition includes combination of several vitamins as main medicinal component (called functional component for health-care food), filling agent, disintegrant, corrective and lubricant. Said oral disintegrant tablet can effectively supplement several vitamins necessary for human body.
EP2275141A1 Tastemasked pharmaceutical compositions A granular pharmaceutical composition, comprising (A) a drug having disagreeable taste; (B) one or more of waxy substances selected from the group consisting of hydrogenated castor oil, hydrogenated soybean oil, hydrogenated rape seed oil, hydrogenated cotton seed oil, camauba wax, white bees wax, beef tallow, stearyl alcohol, cetanol, polyethylene glycol, stearic acid, parmitic acid, mono-fatty acid glycerin ester, tri-fatty acid glycerin ester and fatty acid sucrose ester; and (C) erythritol, characterized in that the composition thereof does not cohere in water and has a dosage form of a granule, powder or capsule.
US7323470 2-Heterocyclyl- indole, pyrrolopyridine, pyrrolopyrimidine, or pyrrolopirazine substituted with an N-(amino)sulfonyl(thio)carboxamide: 3-Cyclohexyl-2-furan-3-yl-7-methyl-1H-indole-6-(N-methylsulfonyl)carboxamide; treating a hepatitis virus infection An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.
CA2303447C Cationic polymers as toxin-binding agents A method for treating pathogenic toxins in a mammal, such as a human, comprising treating the mammal with a therapeutically effective amount of a polymer comprising a cationic group attached to the polymer backbone. The polymer can be a homopolymer or a copolymer. In one embodiment, the polymer is a copolymer comprising a monomer having a pendant ammonium group and a hydrophobic monomer.
WO2011129494A1 Nucleolin specific aptamer and use thereof Improved G-rich oligonucleotide (GRO) aptamers specific to nucleolin, a method of preparing the aptamers, and a use of the aptamers for diagnosing and/or treating a nucleolin-associated disease, are provided.
US20090280987 Method For Solubilising, Dispersing and Stabilising of Substances, Products Manufactured According To The Method As Well As The Use Thereof Disclosed is a method in which poloxamer, a resin, and/or a tocopherol is/are fused, and the material that is to be treated is intimately dispersed with said melt. After being introduced into the melt, the material that is to be treated is coated with water to prevent hardening, and the spontaneously forming gel is homogenized. The obtained product is composed of a transparent gel that is based on at least one poloxamer, a resin or a tocopherol, and an active substance which is solubilized, dispersed, and stabilized therein and whose consistency ranges from solid, semisolid, i.e. aspic-like, to liquid. The micelles of said solubilized matter remain stable even when the same is diluted well below the CMC of poloxamer. The inventive products can be used for dissolving fats, peptides, resins, and all types of resinous materials, removing fats, peptides, resins, and all types of resinous materials from surfaces, cleaning, and lubricating, according to the solubilized active substances used. If a vegetable substance is intimately dispersed in such a melt, the melt is cooled instead of being coated with water. The melt turns brittle and can then be coarsely chopped and ground in a chopper-grinder without producing dust and can then be finely ground in a wet state with water in a hammer mill or an emulsifying mill until the crystals of the melt have been reduced to a diameter of less than 5 micrometers. The crystals of the melt are then dissolved or dispersed in additional water and are added to the humus soil in order for the crystals to be absorbed by the plant via the roots thereof, or the crystals are sprayed directly to the part of the plant that lies above the ground.
CN101897678A Sustained-release composition of cefaclor The invention relates to the technical field of drug release, in particular to a novel sustained-release composition of cefaclor. The sustained-release composition of cefaclor comprises 60-90% of cefaclor, 5-25% of water-soluble adhesives, 0.5-5% of water-insoluble retardants, 2-10% of porogenic agents and 2-15% of cellulose derivatives with water viscosity being more than 500mmPa.s by total weight of the composition. The sustained-release composition of cefaclor can be completely released within 4-8h, has sustained-release effect in bodies and is applicable to administration twice a day.
CN103599109A Application of prednisone and hydroxychloroquine to preparation of compound anti-inflammatory drug The invention discloses an application of prednisone and hydroxychloroquine to the preparation of a compound anti-inflammatory drug. The total dose of prednisone is 0.05-2mg/kg, and the total dose of hydroxychloroquine is 0.83-26.64mg/kg. The prednisone for a mouse, the dose of which is equivalent to half of the normal dose of the prednisone for an adult, is unobvious in anti-inflammatory effect in a dimethylbenzene caused mouse ear swelling test, and the prednisone with the dose has an obvious anti-inflammatory effect after being used together with the hydroxychloroquine. Cell and molecular biological tests prove that IL-1beta and IL-6 transcriptions induced by LPS (Lipopolysaccharide) can be remarkably inhibited by the combination of the hydroxychloroquine and the prednisone, and the inhibiting effect is stronger than the inhibiting effect of the prednisone or the hydroxychloroquine. The invention also develops a novel compound anti-inflammatory drug and lays the foundation for reducing the side treating effect of the prednisone and widening the application range of the prednisone.
US7084148 Analgesics; antipyretics; antiinflammatory agents A compound of formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1 is H or C1-6alkyl; R2 is wherein defines the point of attachment of the ring; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of pain, fever, inflammation of a variety of conditions and diseases.
WO2013172725A1 The use of chitosan polymer in the treatment and prevention of infections caused by coronaviruses The use of chitosan polymers of formula (I), wherein R is selected from H, COCH3 (HTCC) or from H, COCH3, C12H25 (HM-HTCC) in the treatment and prevention of infections caused by coronaviruses.
CN103446157A Compound amino acid-vitamin capsule and preparation method thereof The invention relates to a compound amino acid-vitamin capsule taken twice in a day, and a preparation method thereof. According to the method, the active components include 11 amino acids and 6 vitamins; a proper amino acid stabilizer is added; hydrophilic lactose and microcrystalline cellulose with good forming property are used as diluents; an extrusion-spheronization technology is used for preparing wet granules; a fluidized bed coating technique is used for coating the wet granules, so as to respectively prepare granules of three different colors; the granules are filled into hard capsules. The stability of the preparation can be improved since the three types of granules are prepared separately. The compound amino acid-vitamin capsule is mainly applied to adjunctive treatment of hypoproteinemia caused by various diseases and nutritional supplementation for postoperation or malignant tumors. The compound amino acid-vitamin capsule disclosed by the invention is simple in preparation technology and can be put into large-scale production easily.
EP1551420A1 Aryl phosphate derivatives with selective activity against adenovirus and hiv Methods and compositions for treating ADV infections and HIV/ADV co-infections by administering an aryl phosphate derivative of d4T having an electron withdrawing substituent on the aryl group and an amino acid substituent on the phosphate group are described. Preferred aryl phosphate derivatives of d4T are d4T-5'-[p-bromophenyl methodyalaninyl phosphate] and d4T-5'-[p-chlorophenyl methoxyalaninyl phosphate].
WO2007142923A1 Mif inhibitors for treating neuropathic pain and associated syndromes Methods of using MIF inhibitors such as those characterized by structure I are disclosed. The MIF inhibitors can be used for treating conditions such as neuropathic pain and its associated symptoms, as well as for treating drug and behavioral addictions, such as opiate dependence. Additionally, MIF inhibitor compounds can be used for treating withdrawal syndromes after discontinuance of addictive drug use or behavior.
CN101186563A 3,5-dimethoxyl or 3,5-dihydroxy diphenylethene compounds and preparation method thereof The invention relates to a 3, 5-dimethoxy or 3, 5-dihydric diphenylethene-like compound and a preparation method, pertaining to the organic chemistry and pharmaceutical chemistry fields. A general formula is demonstrated as formula (1). The invention adopts 3, 5-dimethoxy benzyl bromide as raw materials and obtains the 3, 5-dimethoxy or 3, 5-dihydric diphenylethene-like compound through substitution reaction, Witting-Hornor condensation reaction, reduction reaction and iodination reaction. The product of the invention is a novel self designed and synthesized compound, which is applicable to the medical fields of antitumor action, antioxidation, antibacterium, etc.
CN102670981A External medicine for treating burn The invention relates to external medicine for treating burn. Burning and scalding are emergency conditions in people's lives, and wounded people often randomly use substitutes of cold water or toothpaste and the like to treat wounds when wounded. However, the method of using the substitutes is only a temporary treatment method. During the post treatment, the wounded people always buy burning products sold in the market for treatment, most of the burning products are ointment, the used burning and scaling ointment drugs for treatment are poor in effects and prone to cause infections to the wounds if the drugs are used three times a day, and the healing of the wounds is not facilitated.
US20090258921 Indole derivatives Novel indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is halogen, or alkyl, R2 is hydrogen, or halogen, Ar is phenyl, or thienyl, which may be substituted with halogen, alkyl, alkoxy, alkylthio, etc.
CN102327284A Liquid-phase synthesis method of silver-chitosan and/or chitosan derivative nanocomposite The invention discloses a liquid-phase synthesis method of silver-chitosan and/or chitosan derivative nanocomposite. The obtained product has the functions of promoting wound surface healing, arresting bleeding, relieving pain, resisting inflammation and sterilizing bacteria, is suitable for female vaginitis, cervicitis, cervical erosion, bedsore, dermal ulcer, burn, scald, trauma, other skin phlogosis, tinea of feet and hands and the like, and can also be used for preparing various trauma dressings such as thin films, sponges, suppositories for gynecology, application films and the like.
CN101429164A Levorotation benzhydryl piperazidine derivant and preparing method thereof The invention provides a levo-benzhydryl piperazine derivative, which is characterized in that the corresponding general formula of the derivative is as right, wherein X1 represents halogen; n1 is 1 to 5; R1 is H, pyridazinyl or substituted pyridazinyl, purimidyl or substituted purimidyl, and thiazolyl or substituted thiazolyl; and R2 is carboxylic alkyl, p-sulphonyl aniline or p-sulphonyl aniline derivative, and p-amino phenyl sulphonyl. The levo-benzhydryl piperazine derivative is expected to become a long-acting effective levo-antihistamine medicine, and provides one more treatment choice for allergic disease patients.
US20120244120 Inhibitors of hemopoietic cell kinase (p59-hck) and their use in the treatment of influenza infection The present invention relates inter alia to the treatment or prevention of influenza virus infection (including subtypes influenza A virus, influenza B virus, avian strain H5N1, A/H1N1, H3N2 and/or pandemic influenza) using compounds which inhibit the activity of p59-HCK and to a method of screening for a candidate drug substance intended to prevent or treat influenza virus infection in a subject, said method comprising identifying a test substance capable of inhibiting p59-HCK activity.
CN101912616B Alpha-tocopheryl mesoporous silicon compound using supercritical CO2 injection method and preparation method thereof The invention discloses an alpha-tocopheryl mesoporous silicon compound using a supercritical CO2 injection method and a preparation method thereof, belonging to the technical field of medicines. The preparation method comprises a step of preparing alpha-tocopheryl and mesoporous silicon into the alpha-tocopheryl mesoporous silicon compound under the environment of carbon dioxide by means of the supercritical carbon dioxide injection method. The drug-loading rate of the compound prepared by using the method of the invention is 0.58-0.76g/g. The alpha-tocopheryl/mesoporous silicon compound prepared by using the supercritical CO2 injection method can be prepared into food additives with various functions. The process has the advantages of simple process for preparing the compound, high drug-loading rate and no solvent residues, and the compound is a solid formulation.
CN101407460A Trihydroxy-2-acyl phenylacetate, and preparation and use thereof The invention relates to trihydroxy-2-acyl phenylacetic acid easter, a preparation method and the application thereof, which relates to a compound containing trihydroxy-2-acyl phenylacetic acid easter structure, and provides trihydroxy-2-acyl phenylacetic acid easter with novel structure, the preparation method and the application thereof. Starting from gallic acid, firstly, trihydroxy is protected by halogenated hydrocarbon; then, a jarful three-step reaction of acyl chloride-diazotization-Wolff rearrangement is used for getting aryl acetate 4 with one added carbon atom; under the effect of polyphosphoric acid, 4 is reacted with carboxylic acid R<2>CO2H to get acylation product 5; finally, through the effect of catalytic hydrogenolysis or AlCl3, the protecting group is removed to get trihydroxy-2-acyl-phenylacetic acid easter CsT. Moreover, a method of acid-catalyzed transesterification can also be adopted to prepare trihydroxy-2-acyl-phenylacetic acid easter CsT which can function as a primer of antitumor drugs or other active drugs. The preparation method is characterized in that the reagent is easy to get; the operation is simple; and the yield coefficient is relatively high.
US20130053406 Therapeutic compounds and uses thereof The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders such as cancer.
WO2008049401A2 Nail varnish for cosmetic and medical applications The invention relates to a cosmetic and medical nail varnish containing urea, dexpanthenol, a solvent and at least one oil having a weight proportion of more than 20% by wt. of fatty acids containing 10 - 25 carbon atoms. Other components can be added to said composition, such as substances with an anti-mycotic, anti-viral, anti-bacterial, anti-septic, anti-microbial, anti-infectious, anti-psoriatic and/or antiparasitic action. The invention also relates to the use of said type of nail varnish for treating nail diseases and nail infections.
CN103458884A Methods and compositions for treating kidney disorders The present invention provides methods for treating glomerulosclerosis such as focal segmental glomerulosclerosis (FSGS) or glomerulonephritis such as immunoglobulin A nephropathy (IgAN) by cyclohexenone compounds.
EP2077263A1 Quinazolines and related heterocyclic compounds and their therapeutic use A compound of the formula wherein X is CR1 or N; Y is CR3 or N; R1, R3, R4, R5 and R6 are independently H, F, Cl, Br, I, or a hydrocarbon group which optionally contains one or more heteroatoms; R7 is a heterocyclic group including one or more N atoms; R' is Rx or NRyRz wherein Rx, Ry and Rz are each H or the same or different groups, including cyclic groups formed by Ry and Rz with the N atom, of up to 20 C atoms and optionally including up to 3 further heteroatoms selected from N, O and S; or a pharmaceutically acceptable salt, ester or solvate thereof, has therapeutic utility.
WO2011095452A1 Aryl benzylamine compounds The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
CN102579474A Combination with orientin-2''-O-beta-L-galactoside as main ingredient and use of combination The invention relates to a medicine combination which has functions of heat clearing and detoxifying, antisepsis and anti-inflammation, and is used for curing diseases such as upper respiratory tract infection, pharyngitis, tonsillitis caused by wind-heat toxin to the lung and internal exuberance of toxic heat. The medicine combination is extracted and prepared from the dry flowers of ranunculaceae Chinese globeflower plants, such as trollius chinensis bunge, trollius ledebouri reichb and trollius macropetalus Fr. Schmidt. The combination with orientin-2''-O-beta-L-galactoside as the main ingredient has the characteristics of clear effective ingredient, high content and small dose, makes up the defects of the Chinese globeflower oral preparation sold in the existing market. The medicine preparation of the combination is described, and can be anyone preparation of tablets, capsules, pills, granules, suspensoids and suppositories rectal administration.
EP1902721A1 Ernährungs- und medizinische Zusammensetzungen enthaltend Vaccinium macrocarpon Antibacterial composition comprises combination of a Vaccinium macrocarpon extract and an antibacterial active agent against gram positive bacteria and gram negative bacteria such as Escherichia coli, Proteus, Klebsiella and Enterobacter in an excipient or non-toxic inert vehicle. - ACTIVITY : Antimicrobial; Uropathic. - MECHANISM OF ACTION : None given.
CN103536531A Preparation method of long-acting injection containing danofloxacin mesylate The invention relates to an application of sucrose acetate iso-butyrate to preparation of an oil injection for livestock, and in particular relates to a method used for preparing a long-acting injection containing danofloxacin mesylate by combining sucrose acetate iso-butyrate and hydrogenated castor oil or aluminium stearate. A dispersion medium of the preparation is isopropyl myristate, benzyl benzoate, ethyl oleate or a mixture of more than one of isopropyl myristate, benzyl benzoate and ethyl oleate. The preparation has good sustained release effects, stable characters and good tissue compatibility and is easy to prepare.
CN103405469A Microcrystalline cellulose for prevention and treatment on respiratory infectious diseases The invention relates to microcrystalline cellulose for prevention and treatment on respiratory infectious diseases. The microcrystalline cellulose can be processed into preparations suitable for oral administration and nasal delivery, and can be used for preventing and treating respiratory infectious diseases. The microcrystalline cellulose is a strong polar adsorbent, can adsorb viruses and bacteria having strong polarity easily, and can make the pathogens fast lose viability and pathogenicity. An experiment proves that the microcrystalline cellulose can effectively prevent and treat respiratory infectious diseases. After application, the microcrystalline cellulose can fast cure early stage symptoms such as lassitude, cold intolerance and cold feel. The microcrystalline cellulose can treat bacterium-caused inflammation without a fever and respiratory system symptoms. The microcrystalline cellulose can resist virus degeneration and bacterium mutation, has no adverse reaction and toxicity, and is absolutely safe. The microcrystalline cellulose has no odor, no smell, no irritation, good mouthfeel, good compliance and a simple use method, can be manufactured easily, is cheap and can satisfy supply requirements in an epidemic period.
WO2010076333A1 Novel use of fibrates The present invention, which is applicable in the pharmaceutical industry, relates to the use of fibrates, in particular fenofibrate, especially in the form of a solid oral composition, for the manufacture of a drug for the treatment of sleep apnea, sleep apnea syndrome, in particular obstructive sleep apnea or obstructive sleep apnea syndrome.
CN102961437A Pharmaceutical composition containing sophora alopecuroide oil and preparation method thereof The invention relates to a pharmaceutical composition containing sophora alopecuroide oil and a preparation method thereof. The pharmaceutical composition provided by the invention is prepared from sophora alopecuroide and sophocarpidine which are used as raw materials. The preparation method of the pharmaceutical composition comprises the following steps of: performing destructive distillation on the sophora alopecuroide to obtain destructive distillation oil; mixing the sophocarpidine with the destructive distillation oil; adding polysorbate-80 into the mixture, stirring evenly, and then adding osmanthus flower fragrance, ethanol and a proper amount of water into the mixture, and then grinding the mixture through a colloid mill. The sophora-alopecuroide pharmaceutical composition provided by the invention has certain curative effects of detumescence, proliferation inhibition and the like on acute eczema, and is superior to the conventional sophora alopecuroide oil linimentum in anti-pruritus effect; the sophora-alopecuroide pharmaceutical composition also has certain curative effects of detumescence, proliferation inhibition and the like on chronic eczema; and besides, the sophora-alopecuroide pharmaceutical composition has certain antiphlogosis and skin tissue repair effects on dermatitis induced by the chronic eczema, and is superior to the sophora alopecuroide oil linimentum in curative effect.
CN102370654A Inhalation pharmaceutical composition with eplerenone and momestasone furoate as active components An inhalation pharmaceutical composition with eplerenone and momestasone furoate as active components comprises eplerenone, momestasone furoate and one or more carriers suitable for inhalation drug delivery. The inhalation pharmaceutical composition is preferably prepared into a dry powder inhalation, is composed of eplerenone, momestasone furoate and carrier micropowders, wherein the average particle size of the eplerenone and momestasone furoate micropowders is 0.5-10 microns, and the average particle size of the carrier micropowder is 20-45 microns.
US7241887 3-azabicyclo[3.2.1]octane derivatives The subject invention relates to 3-azabicyclo[3.2.1]octane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by opioid receptors. The subject invention also particularly relates to using such derivatives to treat certain disorders and conditions, for example irritable bowel syndrome, drug addiction, depression, anxiety, schizophrenia and eating disorders, among others.
US7135195 Colorless antimicrobioal aqueous suspension of colloidal silver particles having an interior of elemental silver and a surface of silver oxide of given particle diameters; antiseptic and surface disinfectant and for treatment of viral, fungal, and bacterial infections We disclose a colorless composition comprising silver particles and water, wherein said particles comprise an interior of elemental silver and an exterior of ionic silver oxide, wherein the silver particles are present in the water at a level of about 5–40 ppm, and wherein the composition manifests significant antimicrobial properties. Methods of use of the composition are described.
US20100247525 Compositions and methods for treating anthrax lethality The present invention provides compositions and methods for preventing and inhibiting anthrax lethality. The present invention relates to protect a subject from anthrax lethality by presensitizing a subject prior to anthrax infection. The present invention further provides compositions and methods for enhancing the innate system to inhibit anthrax-associated lethality. The invention further provides compositions and methods for preventing and inhibiting lethality due to infection regulated via a TNF-α pathway.
CN101389628A Indolopyridines as EG5 kinesin modulators Compounds of a certain formula (I), in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.
CN102210680A Sinomenine derivatives for treating inflammatory disease by blocking macrophage p38 MAPK (mitogen activated protein kinase) signal transduction pathway The invention discloses an application of sinomenine derivatives as shown in a formula I, which can be used for preparing an inflammatory cell factor activity inhibitor, or preparing a macrophage p38 MAPK (mitogen activated protein kinase) signal transduction pathway blocking agent, and also preparing a composition for preventing and/or treating inflammatory disease and/or autoimmune disease.
CN100584381C Medicinal composition containing sulfourea antidiabetic medicine and vitamine B A composite medicine for treating diabetes and preventing its complication contains antidiabetic sulfonylurea medicine or its metabolite or its salt, one or more vitamins in family B, and medicinal carrier.
WO2008007113A2 Pharmaceutical combinations The invention provides a combination comprising an ancillary compound and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C=O, NR9(C=O) or 0(C=O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy; or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy.
EP0730606B1 Hu-B1.219, A NOVEL HUMAN HEMATOPOIETIN RECEPTOR The present invention relates to a novel member of the hematopoietin receptor family, herein referred to as Hu-B1.219. In particular, the invention relates to nucleotide sequences and expression vectors encoding Hu-B1.219 gene product. Genetically engineered host cells that express the Hu-B1.219 coding sequence may be used to evaluate and screen for ligands or drugs involved in Hu-B1.219 interaction and regulation. Since Hu-B1.219 expression has been detected in certain human fetal tissues and cancer cells, molecular probes designed from its nucleotide sequence may be useful for prenatal testing and cancer diagnosis.
US20080193509 Liposome Preparation Containing Slightly Water-Soluble Camptothecin The present invention aims at providing a slightly water-soluble camptothecin liposome preparation with an excellent retention in blood for a drug, which can stably hold a slightly water-soluble camptothecin compound for a long period of time, whereby hydrolysis of an α-hydroxylactone ring in blood is suppressed and the slightly water-soluble camptothecin compound is kept in a structure in which the ring is not opened and which makes the compound effective as an antitumor-active drug, and, moreover, the liability of the drug to leave a liposome is advantageously reduced, so that it is possible to maintain the drug concentration in plasma for a long period of time after administration. This object is achieved by the liposome preparation as described in the specification. The liposome preparation according to the present invention includes a liposome preparation including as lipid components for forming a membrane a phospholipid and a fatty acid, and containing as a drug a lightly water-soluble camptothecin compound.
WO2011012855A3 Antibacterial combinations comprising a garlic extract or s -allyl cysteine Compositions and their use for treating bacterial infections are described, in particular compositions for treating multi-species infections and the treatment of bacterial infections arising from biofilms. The present invention also relates to antibacterial compositions for treating dental diseases. Compositions of the present invention may include a garlic extract or S-allyl cysteine, and optionally an antibiotic and/or an antiseptic.
WO2011026835A1 Novel pyrimidine and triazine hepcidine antagonists The present invention relates to novel hepcidine antagonists of the formula (I), comprising pharmaceutical compositions and the use thereof as medications, in particular for treating iron metabolism disorders, such as in particular iron deficiency diseases and anemias, in particular anemias in conjunction with chronic inflammatory diseases (ACD, anemia of chronic disease, and AI, anemia of inflammation).
EP0673241B1 Use of a free radical quenching liposomal composition for the manufacture of a medicament for the treatment of inflammatory conditions A free radical quenching composition is disclosed comprising a liposome containing at least two antioxidants selected from the following group: beta-carotene, vitamin E, vitamin C, glutathione, niacin, and optionally at least one trace metal (Zn, Se, Cr, Cu, Mn). Also disclosed is a method for reducing the undesirable side effects of free radicals in a mammal by administering to a mammal in need of such antioxidants an effective amount of liposomes containing at least two antioxidants.
WO2014033314A1 Antisense oligonucleotide targeting bacterial glucosyltransferases The present invention provides isolated antisense oligonucleotides (ASO) and methods for reducing, preventing or inhibiting biofilm formation such as biofilm in the oral cavity. The present invention further provides compositions such as pharmaceutical compositions comprising said ASO.
US7173053 effective against the growing number of resistant bacteria, particularly the vancomycin resistant enterococci and beta -lactam antibiotic-resistant bacteria, such as methicillin-resistant Staphylococcus aureus Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(═O) or formula C(═O)NH(OH); R1 represents hydrogen, methyl or trifluromethyl, or except when Z is a radical of formula —N(OH)(═O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1–C6) alkyl or phenyl(C1–C6)alkyl-; and R5 and R6 are as defined in the specification.
US7776908 Use in inhibiting PI-3-kinase activity in mammals; cancer; Acetic acid 4-diallylaminomethylene-6-hydroxy-1- alpha -methoxymeth-yl-10 beta ,13 beta -dimethyl-3,7,17-trioxo-1,3,4,7,10,11 beta , 12,13,14 alpha ,15,16,17-dodecahydro-2-oxa-cyclopenta[ alpha ]phenanthren-11-yl ester Novel Wortmannin analogs and their use in inhibiting inhibiting PI-3-kinase activity in mammals as well, as tumor formation in a subject are described herein.
WO2011089995A1 Hydroxamic acid derivative and hdac8 inhibitor using same Disclosed are: a compound which is capable of inhibiting the function of HDAC8; and an HDAC8 inhibitor. Specifically disclosed is a hydroxamic acid derivative which is characterized by being composed of a compound represented by general formula (1) (wherein X represents an aromatic substituent or an optionally substituted 3-8 membered ring, and n represents an integer of 0-20), or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof.
US7041824 Such as trans-N2-(4-aminocyclohexyl)-N6-(2-aminoethyl)-1H-purine-2,6-diamine trihydrochloride for treatment/prevention of fungal diseases The use of purine derivatives of formula (I): in which: Rx is —(Z)n—R1 wherein Z is a divalent radical selected from —CH2—, —SO2—, —CO—, —COO—, —CONH— and —(CH2)2—NR6—, n is the an integer selected from 0 and 1, R1 is selected from hydrogen, aryl, —CH2-aryl, —SO2-aryl, heterocyclic, —CH2-heterocyclic, alkyl and —SO2-alkyl, Ry is a phenyl radical (optionally substituted) or the radical: wherein D1 and D2, which are identical or different are selected from hydrogen, hydroxyl, the linear or branched alkyl or alkoxy radicals containing at most 6 carbon atoms and NHR5, or, alternatively, taken together, D1 and D2 form a radical selected from ═O and ═N—OR4, R4 is hydrogen, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl or aryl, R5 is hydrogen, alkyl, cycloalkyl, or —COOtBu (Boc), and R6 is hydrogen, alkyl or cycloalkyl, wherein the alkyl moiety contains 1 to 6, optionally substituted, carbon atoms; as cdk kinase inhibitors for the prevention and treatment of fungal infections. Also disclosed are novel methods and intermediates for the production of compounds of formula I, as well as pharmaceutical compositions containing said compounds.
EP1140136B1 Compositions and methods for the prevention or treatment of cancer and bone loss associated with cancer The present invention relates to compositions and methods for the prevention and/or treatment of bone loss associated with cancer. More particularly, the invention relates to OPG compositions and methods for the prevention and/or treatment of bone loss comprising said compositions. The invention also relates to the use of OPG compositions for the treatment of multiple myeloma.
US7375136 Such as 1-(4-methanesulphonamidepheoxy)3-(N-methyl-3,4-dichlorophenylethylamino)-2-propanol; synthesis; effective against brain and/or spinal cord tissue acidification disorders NMDA receptor blockers, including pH-sensitive NMDA receptor blockers, are provided as neuroprotective drugs that are useful in stroke, traumatic brain injury, epilepsy, and other neurologic events that involve acidification of brain or spinal cord tissue. Compositions and methods of this invention are used for treating neurodegeneration resulting from NMDA receptor activation. The compounds described herein have enhanced activity in brain tissue having lower-than normal pH due to pathological conditions such as hypoxia resulting from stroke, traumatic brain injury, global ischemia that may occur during cardiac surgery, hypoxia that may occur following cessation of breathing, pre-eclampsia, spinal cord trauma, epilepsy, chronic pain, vascular dementia and glioma tumors. Compounds described herein are also useful in preventing neurodegeneration in patients with Parkinson's Alzheimer's, Huntington's chorea, ALS, and other neurodegenerative conditions known to the art to be responsive to treatment using NMDA receptor blockers. Preferably the compounds provided herein are allosteric NMDA inhibitors.
CN102860992A Tiacumicins B sustained release or controlled release composition orally taken for one time per day The invention provides a tiacumicins B-containing medicinal composition which can be orally taken. The composition comprises tiacumicins B and at least one excipient, wherein the tiacumicins B has effective dosage for treatment and can be used as a medicament; and the excipient can be used as a medicament. When the releasing rate of the composition is detected by releasing rate detecting equipment and a releasing rate detecting universal condition in the Appendix II of the 2010 edition of 'Chinese Pharmacopoeia', at the first hour, the fourth hour and the twelfth hour after detection, the composition has the following characteristics that: 1, the detected releasing rate is in the range of 10 to 35 percent of marked dosage when sampling is performed at the first hour after detection; 2, the detected releasing rate is in the range of 30 to 60 percent of marked dosage when sampling is performed at the fourth hour after detection; and 3, the detected releasing rate is not less than 70 percent of marked dosage when sampling is performed at the twelfth hour after detection.
US20080319045 Combination of Histone Deacetylase Inhibitors and Radiation This invention relates to organic compounds of formula (I): in particular, to pharmaceutical compositions for use in combination with ionizing radiation for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease.
CN102670532A Iloperidone medicine composition and preparation method thereof The invention belongs to the technical field of iloperidone medicine preparations. In the iloperidone medicine composition provided by the invention, the auxiliary medicines include two or more disintegrating agents; the iloperidone exists in the form of particles; and the particle size of at least 90% of the particles is less than 50mm, most preferably less than 20mm. In the invention, the dissolution rate of the medicine in 5 minutes can be improved by using composite disintegrating agents and controlling the particle size, the aim of fast dissolution of the medicine is achieved, and the medicine takes an effect quickly.
EP1758651A2 Lxr agonists to promote bone homeostasis The present invention relates to a method for promoting osteogenesis by contacting osteoblast progenitor cells with an LXR agonist. Said method is useful for the treatment or prevention of an imbalance in bone homeostasis in a subject using bone homeostasis-promoting compositions comprising an effective osteogenic stimulating amount of an LXR agonist in admixture with a pharmaceutically acceptable carrier. A further aspect is a method to produce bone tissue in vitro by contacting an LXR agonist with a population of osteoblast progenitor cells on a substrate, for a time sufficient to stimulate the generation of a matrix of bone tissue.
WO2010093601A1 Novel sulfonic acid-containing thyromimetics, and methods for their use The present invention relates to sulfonic acid containing compounds of formula IB, in which G, R1, R3 and T are as defined in the claims, that bind to thyroid receptors in the liver. Activation of these receptors results in modulation of gene expression of genes regulated by thyroid hormones. The compounds can be used to treat diseases and disorders including metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome X and diabetes.
US20070203063 Pharmaceutical compositions including variants of vascular endothelial cell growth factor having altererd pharmacological properties Described herein are pharmaceutical compositions including vascular endothelial cell growth factor (VEGF) variants having modifications in the C-terminal heparin binding domain. The variants exhibit reduced clearance rates for systemic administration generally at lower doses compared with native VEGF thus providing variants having longer availability for therapeutic effect.
US6870042 Mutants of streptococcal toxin A and methods of use This invention is directed to mutant SPE-A toxins or fragments thereof, vaccine and pharmaceutical compositions, and methods of using the vaccine and pharmaceutical compositions. The preferred SPE-A toxin has at least one amino acid change and is substantially non-lethal compared with the wild type SPE-A toxin. The mutant SPE-A toxins can form vaccine compositions useful to protect animals against the biological activities of wild type SPE-A toxin.
WO2009019472A1 1, 2, 4 -triazole derivatives as serotonergic modulators The invention relates to novel 5-hydroxytryptamine (5-HT) receptor modulator compounds of formula (I); wherein A, B, R1-R5, T, W, X, Y, Z and m are defined herein, to pharmaceutical compositions comprising these compounds and to their use in the treatment of conditions associated with 5-HT action.
CN101309920A Novel method for producing tiotropium salts The invention relates to a novel method for producing tiotropium salts of formula (I), wherein X can have significances specified in claims and a description.
US20120077834 Methods of Use of Cyclopamine Analogs The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:
CN101244068A Hemsleyadin sustained-release preparation The invention relates to a special sustained-release preparation of natural antibiotics curcurbitacin, in particular to a membrane controlled or/and matrix release oral preparation with the composition as follows: curcurbitacin 5 to 20%, water insoluble medical macromolecular material 30 to 65%, water soluble medical macromolecular material 5 to 25%, and conventional auxiliary material 15 to 45%. The special sustained-release preparation of natural antibiotics curcurbitacin has the advantages of retarding the release of curcurbitacin from drug preparation, reducing the peak and peak valley for drug absorption, facilitating stable plasma drug concentration, and especially facilitating the disease treatment when the sustained release is combined with rapid release since the rapid release part can be rapidly released to produce the plasma drug concentration required for treatment as soon as possible, while the sustained release part can subsequently provide stable plasma drug concentration and reduce the fluctuation of plasma drug concentration.
US20100249228 Sarms and method of use thereof This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds.
US20110129519 Modafinil-Based Treatment For Premature Ejaculation Methods and compositions comprising modafinil are described for treating premature ejaculation in a male individual.
US20110288062 Biodegradable polymer system A polymer system useful for in vivo delivery of a therapeutic agent is provided. The polymer system comprises a biocompatible biodegradable polymeric backbone that is capable of a reversible stimuli-induced transition from liquid to gel.
US20090105203 Compounds for treating viral infections The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.
WO2009007987A1 An improved process for the preparation of alfuzosin and its novel polymorph The present invention relates to an improved process for the preparation of Alfuzosin of formula (I). The process involves utilizing intermediate of formula (Ia) wherein S represents acid residue of organic acids like acetic acid, oxalic acid, succinic acid, methane sulfonic acid, p-toluene sulfonic acid and the like. The present invention also relates to novel Amorphous form of Alfuzosin of formula (I).
US7101853 Provided amylin agonist is not calcitonin; also amylin used in combination with an nonsteroidal antiinflammatory agent to relieve pain, thereby achieving a synergistic effect Methods for treating or preventing gastritis or gastric injury are disclosed, comprising administering a therapeutically effective amount of an amylin or an amylin agonist. Methods are also disclosed for the treatment of pain, fever, inflammation, arthritis, hypercoagulability, or other conditions for which a non-steroidal anti-inflammatory drug would be indicated, comprising administering an amylin or amylin agonist in conjunction with administering a therapeutically effective amount of a non-steroidal anti-inflammatory agent. Pharmaceutical compositions comprising an amylin or amylin agonist and a non-steroidal anti-inflammatory drug are also disclosed.
CN1562014A V emulsion nicotinate for injection and its preparing method A VE nicotinate injection in the form of emulsion for preventing cerebral infarction is prepared from VE nicotinate, oil for injection, glycerine, emulsifier, coemulsifier and pH regulator. Its preparing process is also disclosed.
EP1049679B1 Sulphonamide derivatives for treatment of cns disorders The invention relates to novel compounds of formula (I) or a salt thereof: in which the group D is selected from a group of formula (A), (B) or (C). Compounds of formula (I) and their pharmaceutically acceptable salts have 5HT6 receptor antagonist activity and are believed to be of potential use in the treatment of certain CNS disorders such as anxiety, depression, epilespy, obsessive compulsive disorders, migraine, cognitive memory disorders e.g. Alzheimers disease, Parkinson' Disease, ADHD (Attention Deficit Disorder/Hyperactivity Syndrome), sleep disorders (including disturbances of Circadian rhythym), feeding disorders such as anorexia and bulimia, panic attacks, withdrawal from drug abuse such as cocaine, ethanol, nicotine and benzodiazepines, schizophrenia, and also disorders associated with spinal trauma and/or head injury such as hydrocephalus. Compounds of the invention are also expected to be of use in the treatment of certain GI (gastrointestinal) disorders such as IBS (Irritable Bowel Syndrome).
US20090069428 Catalytic antioxidants and methods of use The invention provides small molecules that act as catalytic antioxidants and methods of use thereof. The compounds can repeatedly bind and destroy reactive oxygen species by serving as substrates for enzymes of the methionine sulfoxide reductase (Msr) class. Some embodiments of the catalytic antioxidant compounds are derived from drugs with anti-inflammatory activity due to inhibition of cyclooxygenase enzymes.
CN101816655A Medicinal preparation containing repaglinide and ligustrazine and application thereof in diabetic complications The invention relates to a unit dosage combination preparation used for the combined delivery of repaglinide and ligustrazine or salts thereof. The preparation can be used for treating diabetic complications such as diabetic nephropathy, diabetic cardiomyopathy and aortic pathological changes, diabetic retinopathy and lenticular pathological changes, diabetic peripheral neuropathy, and the like. The invention also relates to a preparation method of the combined unit dosage preparation and an application of the combination preparation in the treatment of the diabetic complications.
US20080021016 Combined Pharmaceutical Composition for the Inhibition of the Decline of Cognitive Functions The invention relates to a combined pharmaceutical composition for the inhibition of the decline of cognitive functions comprising as A) component (1R,2S,4R)-(-)-2-[N,N-(dimethylaminoethoxy)]-2-phenyl-1,7,7-trimethylbicyclo]-2-phenyl-1.7.-trimethylbicyclo[2.2.1]heptane of the formula (I) or a pharmaceutically acceptable acid addition salt thereof and as B) component a nootropic, an inhibitor of the acetylcholinesterase enzyme and/or a further pharmaceutical active ingredient which exhibits a beneficial effect on the cognitive processes in admixture with suitable inert pharmaceutical carriers and/or auxiliary agents. The combined pharmaceutical composition according to the present invention can be particularly used for the treatment of Alzheimer disease or other diseases showing similar symptoms, diseases accompanied by malfunctions of intellectual abilities (e.g. mental decline in schizophrenia), mental decline in elderly (dementias in elderly), Korsakoff syndrome, Huntington syndrome, Parkinson syndrome or mental decline produced by alcoholism.
CN103751207A Medicinal composition for treating Alzheimer's disease and application thereof The invention belongs to the technical field of medicine, particularly relates to a medicinal composition for treating Alzheimer's disease and application thereof. The medicinal composition comprises is prepared from the following raw materials: Lycium barbarum polysaccharide component III, Lycium barbarum polysaccharide component VI, resveratrol, friedelin-3beta-ol, Astragalus polysaccharide component A2 and Ajugol A. The medicinal composition provided by the invention has obvious therapeutic effect on Alzheimer's disease, has the advantages of stable quality control, low cost, no toxicity and is suitable for long-term administration.
EP0980362B1 Substituted heterocycles and their use in medicaments The invention relates to compounds of formula (I), to the production of said compounds and their use in medicaments.
WO2004087209A9 Preparation for sustaining therapeutically effective blood concentration of analgesic activity potentiator A preparation for enhancing the analgesic effect of an analgesic while avoiding side effects characterized by containing an analgesic activity potentiator and being capable of sustaining the blood concentration of the analgesic potentiator in the steady state at 10 to 150 ng/ml.
CA2782872A1 Compositions and methods for ophthalmic delivery of nasal decongestants The invention provides compositions and methods for treating nasal congestion through ophthalmic delivery. The provided compositions and methods utilize Sow concentrations of selective a-2 adrenergic receptor agonists. The compositions preferably include brimonidine.
WO2006068266A1 PROSTAGLANDIN F2α DERIVATIVE CONTAINING PRODUCTS The invention provides a resin-made container which enables long-term stable preservation of aqueous liquid preparations containing prostaglandin F2α derivatives having fluorine atoms in the molecule. An aqueous liquid preparation containing a prostaglandin F2α derivative having a fluorine atom in the molecule is protected from lowering in the prostaglandin F2α derivative content by keeping the preparation in a container made of a propylene/ethylene copolymer having a propylene/ ethylene ratio of 94.0/6.0 to 99.5/0.5.
US20060161004 Quinoline derivatives for therapy and prophylaxis of chronic obstructive pulmonary disease (COPD), asthma, airway hyper-reactivity, cough, inflammatory diseases such as inflammatory bowel disease, psoriasis, fibrositis, osteoarthritis Certain compounds of formula (I): or a pharmaceutically acceptable salt or hydrate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.
WO2010124873A8 3- (2, 2, 2, trimethylhydrazinium) propionate dihydrate (meldonium) for treating parkinson' s disease Use of Meldonium dihydrate (3-(2,2,2-trimethylhydrazinium)propionate dihydrate) or its pharmaceutically acceptable salts for prevention and/or treatment of Parkinson's disease.
CN101342183A Application of medicament in treating athlete's foot The present invention discloses a medicine for curing athlete's foot. The athlete's foot is caused by the subcutaneous growth and propagation of eumycete. The prior medicine for curing athlete's foot is weak in medicine permeability and poor in curing effect. The medicine provided by the preset invention with strong permeability can deeply extend to the subcutaneous growth place of eumycete so as to prevent the forming of eumycete cellular membrane and the propagation and infection of eumycete. Through tracking and visiting 200 cases of patients who use the medicine provided by the present invention to cure athlete's foot, the effective rate is 100 percent, the curing rate is 98 percent and the curing effect is obvious.
CA2250906C Enteric-coated pharmaceutical compositions of mycophenolate This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.
CA2395980C 10, 11-difluoromethylenedioxycamptothecin compounds with topoisomerase i inhibition Camptothecin compounds having a C10 11 O-(CF2)nO group where n is 1 or 2 are effective anti-tumor compounds. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I-DNA cleavable complex.
US20080146587 for enhancing cognitive memory in an Alzheimer's patient; 5-HT2-selective and 5-HT6 selective ligands Compounds of formula I or formula II: or pharmaceutically acceptable salts thereof, wherein m, n, p, Ar R1, R2, R4, and R5 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds.
CA2732282A1 Aminopropylidene derivative The present invention provides an aminopropylidene derivative represented by the formula (I), having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient such as an antihistamine, having alleviated side effects in the central nervous system, such as drowsiness. In the formula, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid with proviso that a case where both are hydrogen is excluded; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.
WO2011133052A3 Use of the modified polysaccharides for heparin neutralization The subject of the invention is the use of cationically modified polysaccharides, except for chitosan, for direct neutralization of heparin in blood and physiological fluids in a mammal. Cationic modification of the polysaccharides is achieved using compound containing cationic ammonium groups and/or the polysaccharides are grafted with a polymer containing amine and/or ammonium groups.
CN102451377A Preparation method of psoriasis treatment tincture The invention relates to a preparation method of a psoriasis treatment tincture. The preparation method of the psoriasis treatment tincture comprises immersing Chinese gall, bletilla striata and white garden balsam by alcohol in a bottle, pouring out leachate, and adding salicylic acid, benzoic acid and the like into the leachate until full dissolution to obtain the psoriasis treatment tincture. The psoriasis treatment tincture can be smeared on a wounded part. The psoriasis treatment tincture has obvious psoriasis treatment effects.
WO2013000209A1 Use of koumine in preparation of medicament for treatment of rheumatoid arthritis Provided is a use of koumine in preparation of a medicament for treatment of rheumatoid arthritis, and especially, a use of Gelsemium elegans Benth. alkaloid monomer koumine or pharmaceutically acceptable salts thereof in preparation of a medicament for treatment of rheumatoid arthritis.
US20120028954 Substituted Pyridine, Pyridazine, Pyrazine And Pyrimidine Compounds And Methods For Using The Same Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
WO2009109850A3 N-substitutedbenzenepropanamide or benzenepropenamide derivatives for use in the treatment of pain and inflammation Compounds for use in the treatment or prophylaxis of pain, including acute and chronic pain (e.g., nociceptive pain, neuropathic pain, headaches, migraine), represented by general formula (I) in which: the dotted line represents a single or a double bond; and R5 and R5' are independently -H, -OH or -OR6, where R6 is a linear or branched C1-C4 alkyl; X is -0-, -CH2O-, -CH2CH2O-, -CH(CH3)CH2O- or -CH2CH(CH3)O-; Z is -CH2CH2O-, -CH(CH3)CH2O- or -CH2CH(CH3)O-; m is an integer of O or 1; and n is an integer of 0-50. The compounds of the invention are also effective for reducing inflammation and may be used alone or in combination with other analgesics.
CN102178845B Plaster for treating spur and preparation method thereof Spur is a common frequently-occurring disease and is poor in effect and easy to relapse when being treated by adopting common medicines or adopting methods such as manipulation, drawing, physiotherapy, acupuncture, small acupotomy, operation and the like. Aiming at the spur disease pathogenesis, the invention provides a plaster for treating the spur and a preparation method thereof. The plaster comprises the following components: 5-10g of artificial moschus, 15-25g of dragon's blood, 30-60g of angelica root, 18-40g of natural indigo, 30-50g of manchurian wildginger, 20-50g of Chinese ephedra,30-50g of cowherb seed, 40-60g of prepared common monkshood mother root, 40-60g of prepared radix aconiti kusnezoffii, 30-70g of rhizoma corydalis, 30-50g of indian iphigenia bulb, 50-80g of grifola,30-50g of fangchinoline, 45-80g of herba siegesbeckiae, 30-60g of uniflower swisscentaury root, 50-60g of rhizoma homalomenae, 30-65g of medcinal evodia fruit, 40-75g of arisaema with bile, 10-15g ofscorpion, 30-70g of mustard seed, 100-450g of garlic, 10-30g of Japanese buttercup herb, 1000-1500g of sesame oil and 500-1000g of dimethyl sulfoxide. The plaster has the advantages of convenience for use, low cost, no side effects, no drug anaphylaxis reactions, and high cure rate up to 95 percent.
US7803792 benzothiazepine compounds having a thioamide bond and a quaternary ammonium substituent, exhibiti a potent ileal bile acid transporter inhibiting activity, used for for treating hyperlipidemia or arteriosclerosis A method for inhibiting ileal bile acid transporter activity in a subject, comprising administering to said subject an effective amount of a compound represented by formula (1):
CN102199079A Phenol compound and preparation method and application thereof The invention relates to biological pharmacy, in particular to a phenol compound shown in a figure (I) and a preparation method and application thereof. Exophiala pisciphila PHF-9 is a strain of fungus obtained by separating a soil sample, and a compound 1 can be obtained through artificial fermentation culture, separation and purification; and experiments prove that the half-inhibitory concentrations (IC50) of the compound 1 on a human lung adenocarcinoma cell strain A-549, a human pancreatic cancer cell strain PANC-28, a human cervical cancer cell strain Hela and a human liver caner cell strain BEL-7402 are 16, 20, 23 and 30mu g/mL respectively, and the compound 1 has anti-tumor activity and can be used as a cell proliferation inhibitor or tumor cell killing agent.
US7439362 For treatment of acne, seborrhea, androgenic alopecia. hirsutism, and breast cancer Piperazinyl- or piperidinylamine-sulfamic acid amides and their use for the manufacture of a medicament in diseases mediated by the action of steriod sulfatase.
EP1968572A1 Use of benzo-fused heterocycle sulfamide derivatives for the treatment of substance abuse and addiction The present invention is a method for the treatment of alcohol abuse and / or addiction comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and / or formula (II) as herein defined.
US20090069279 Invert emulsions containing dhea Stable, recrystallization-resistant invert emulsions, suited, e.g., for preventing/treating the signs of chronological or actinic skin aging and for preventing/treating atrophy of the skin or mucous membranes, comprise a cosmetically/therapeutically effective amount of DHEA and/or chemical and/or biological precursor or derivative thereof, such invert emulsions also comprising a glycolic or hydroglycolic dispersed hydrophilic phase, a lipophilic continuous phase and an emulsifier having an HLB ranging from 2 to 7.
EP1745797A2 Vascularization inhibitors This invention provides a therapeutic agent for inhibiting neovascularization, a therapeutic agent for a solid cancer, a therapeutic agent for a disease pathologically caused by neovascularization, and a therapeutic agent for repairing a tissue comprising as the effective ingredient, a substance that potentiates the action of CXCR4. Based on the finding that vascularization is suppressed in CXCR4 knockout mice, it becomes possible to prepare a therapeutic agent for suppressing vascularization, a therapeutic agent for a solid cancer, a therapeutic agent for a disease pathologically caused by neovascularization, each of which comprises as the effective ingredient, a substance that inhibits the action of CXCR4, as well as to prepare a therapeutic agent for repairing a tissue comprising as the effective ingredient, a substance that potentiates the action of CXCR4. By using these substances, treatments are made possible.
CN101302511A Nucleic acid molecule NRN1SR12 and use thereof in anti-cancer medicine preparation The invention belongs to the biologic medical field, relating to NRN1SR12 and an application of NRN1SR12 in making an antitumor drug. As health of human is threatened heavily by tumors, the invention provides nucleotide molecule NRN1SR12 for making an antitumor drug. The sequence of the nucleotide molecule comprises 5'-AGAGTTCGAATAAGCTGCC-3' or 5'-AGAGUUCGAAUAAGCUGCC-3'. Compared nude mice containing NRN1SR12 with nude mice containing no-NRN1SR12 under the same culture condition, growth of the tumor body is obviously inhibited and such a phenomenon is increasingly obvious as time goes on. The nucleotide molecule NRN1SR3 for making the antitumor drug provides a new way and a new means for the treatment and release of the tumor.
US20080254099 Pharmaceutical Compositions Comprising Polymeric Binders with Non-Hydrolysable Covalent Bonds and Their Use in Treating Celiac Disease A pharmaceutical composition comprising a polymeric binder including a high molecular weight synthetic polymer having a backbone constituted of non hydrolysable covalent bonds, said polymer being able to form electrostatic bonds at a pH lower than the isoelectric point of gluten and peptides derived from the degradation of gluten, and being able to bind to gluten or peptides derived from the degradation of gluten in the gastrointestinal tract, and a pharmaceutically acceptable carrier. Methods of using the polymeric binder for binding gluten or a peptide derived from the degradation of gluten, for decreasing the degradation of gluten into toxic peptides or for decreasing interaction of gluten or peptides derived from the degradation of gluten with the gastrointestinal mucosa.
CN101332189A Improved gastrodine effervescence tablet and preparation method thereof The present invention relates to a gastrodin effervescent tablet which is assuasive and is used for remedying the insomnia and the cardiovascular neurogenic headache and a preparation method thereof. The present invention aims at providing the wide patient and the medical worker with a new preparation gastrodin effervescent tablet which is disintegrated and absorbed fast, has high bioavailability, is convenient for being taken with less intestinal residues and less side effect. Gastrodin is taken as the raw material, and the specific sorts of accessories in proportion are added. The gastrodin effervescent tablet is prepared by the technical measurement provided by the present invention, and a product of the present invention has sweet flavor with fragrance, takes effect fast, has high bioavailability and is very easy for improving the medication compliance of the patient.
WO2006048331A1 11β-HSD1 INHIBITORS The invention relates to sulfonamide compounds of formula (I) wherein A, B, R1 and Xl to X3 have the meaning as cited in the description and the claims. For example A is biphenyl, B is 3-methoxyphenyl, Rl is H and Xl to X3 are CH. Said compounds are useful as 11 β-HSD1 inhibitors. The invention also relates to the preparation of such compounds as well as the production and use as medicament.
CN102028919A Application of Tibetan medicine composition to preparing medicament for treating fracture The invention discloses application of a Tibetan medicine composition to preparing a medicament for treating fracture, wherein the Tibetan medicine composition comprises the following bulk herbs in parts by weight: 5-15 parts of lamiophlomis rotate, 2-10 parts of whin, 15-60 parts of curcuma, 7-20 parts of pepper, 5-15 parts of cornu bubali, 15-40 parts of myricariagermanica, 0.1-2.5 parts of safflower, 0.1-5 parts of borneol and 0.1-5 parts of camphor. Through the further research of pharmacology of the traditional Tibetan medicine compositions, the Tibetan medicine composition is found to have favorable curative effect on treating the fracture; furthermore, because pure natural wild herbs produced in the Tibet plateau are utilized in the Tibetan medicine composition and no chemical synthetic stabilizer is added, the Tibetan medicine composition does not have toxic or side effect on a human body, is safe and effective, suitable for various kinds of people and adapted to treating various kinds of fractures.
US7875652 Method and composition for treating pain or tinnitus aureum The present invention concerns the novel use of compounds of the Formula I: for treating allodynia as major and unique pain symptom independent of the nature of an underlying disease, but that is often related to neuropathic pain or other different types of chronic or phantom pain.
CN101113447A Antineoplastic small molecule interfering RNA and its anti-tumor use The invention relates to small-molecule antitumor interference RNA and applications thereof. The small-molecule antitumor interference RNA comprises a nucleotide series sense strand of 5'-AGCAUUCGUCCGGUUGCGCX-3' and a nucleotide series antisense strand of 5'-GCGCAACCGGACGAAUGCUX-3', wherein, X stands for tt, TT or UU, t stands for deoxidation thymine. More particularly the invention relates to a structure and antitumor application of the small-molecule interference RNA of apoptotic inhibitant gene surviving. The invention has high-efficiency and universal siRNA antitumor effect and good inhibition effect in vitro on lung cancer, liver cancer, leukemia, gastric cancer, cervical cancer and oral epithelial carcinoma, etc. After the transcription thereof is interfered, CPUsiRNA3 is translated to induce the apoptosis of phyma cells, inhibit phyma cell splitting, reduce drug resistance of phyma cell and inhibit the form of tumor blood vessels and realize to inhibit phyma.
WO2005106492A3 Diagnostics and therapeutics for diseases associated with c-c chemokine receptor 3 (ccr3) The invention provides a human CCR3 which is associated with the cardiovascular disorders, gastrointestinal and liver diseases, metabolic diseases, inflammatory diseases, hematological disorders, respiratory diseases, muscle-skeleton disorders, neurological disorders, urological disorders, cancer disorders and reproduction disorders. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular disorders, gastrointestinal and liver diseases, metabolic diseases, inflammatory diseases, hematological disorders, respiratory diseases, muscle-skeleton disorders, neurological disorders, urological disorders, cancer disorders and reproduction disorders. The invention also features compounds which bind to and/or activate or inhibit the activity of CCR3 as well as pharmaceutical compositions comprising such compounds.
CN101601652A Momestasone furoate lipidosome cream The invention relates to a lipidosome medical composition which uses momestasone furoate as an active component, and a cyst diameter of lipidosome is smaller than 800nm. The composition comprises 0.025 percent to 0.2 percent of momestasone furoate as the active component, 0.5 percent to 6 percent of phospholipid, 0 percent to 1 percent of lipophilic additive, 0.01 percent to 1 percent of antioxidant which is used for preserving the medical composition, a pH buffering agent which is used for retaining a pH value from 5 to 7.5, 3 percent to 15 percent of humectant, 20 percent to 30 percent of oil phrase component, 0.01 percent to 0.1 percent of antimicrobial preservative and the balanced of water. The momestasone furoate lipidosome cream is used for treating skin diseases of human beings or animals.
CN102133390A Calcium tablets and production process The invention discloses calcium tablets and a production process. 100 calcium tablets can be prepared from the following raw materials: 745 grams of calcium carbonate, 200 grams of calcium citrate, 100 grams of casein phosphopeptide, 15 grams of citric acid, 2 grams of orange essence, 80 grams of mannitol, 3 grams of aspartame, 0.1 gram of lemon yellow, 49.9 grams of microcrystalline cellulose and 5 grams of magnesium stearate. The calcium tablets are convenient to eat, do not have side effect and can be easily absorbed by human bodies.
US20080166339 Inhibition of osteopontin for treatment of relapsing autoimmune disease Methods are provided for the inhibition or prevention of relapses in pre-existing autoimmune disease by decreasing activity or expression of osteopontin in immune cells found in tissues affected by the autoimmune disease. Osteopontin is shown herein to mediate autoimmune relapses and induce a shift to the secondary or progressive stage in autoimmune disease. Osteopontin promotes the survival of activated T cells through regulation of transcription factors, FoxO3a and NF-κB and via the expression of pro-apoptotic proteins.
CN1857253A Anticancer injection of rabdosia diterpene compound or its derivative and its preparing method The present invention provides a kind of anticancer injection containing rabdosia diterpene or its derivative and beta-cyclodextrin or its derivative. The insoluble rabdosia diterpene is first prepared into cyclodextrin inclusion to raise the dissolubility, and then prepared into injection or freeze dried powder for injection. The anticancer injection has high stability, high treating effect on liver cancer, esophageal cancer, gastric cancer and other malignant solid tumors and leukemia, and patient's compliance.
US7244767 Therapy for multiple sclerosis, psoriasis, urticaria; antiarthritic agents; incotinence; antitumor, anticancer agents The present invention relates to the use of N-acylvanillinamide derivatives capable of activating the peripheral receptor CB1 of cannabinoids. In particular, the present invention relates to the use of compounds of general formula (I) in which the meanings of R, R1, R3 and Y are as defined in the description, for the preparation of a medicinal product which is capable of activating the peripheral receptor CB1 of cannabinoids.
CN101695489A Aztreonam composition, powder injection and preparation method thereof The invention discloses an aztreonam composition. The composition comprises sterile aztreonam and arginine, and the weight ratio of the sterile aztreonam to the arginine is between 1:1 and 1.5:1. The weight of the sterile aztreonam is based on C13 compound. The aztreonam composition can be used for aztreonam powder injection with good stability and clarity and low water content. The invention also discloses a method for preparing the sterile aztreonam. The method is improved on the basis of the prior art to increase the purity and yield of prepared aztreonam compared with the prior art.
US20090035306 Quinazolinone modulators of tgr5 The present invention relates to quinazolinone compounds useful as modulators of TGR5 and methods for the treatment or prevention of metabolic, cardiovascular, and inflammatory diseases.
CN101584668A Bendamustine hydrochloride freeze-dried powder injection The invention relates to a bendamustine hydrochloride freeze-dried powder injection and its preparing method. The prepared bendamustine hydrochloride freeze-dried powder injection is used for chronic lymphocytic leukemia (CLL) and in the treating process of rituximab/ MabThera or containing the same, or for inert B cell non hodgkin lymphoma (B-NHL) patients whose illness state still deteriorates during the treatment period in six months. The bendamustine hydrochloride freeze-dried powder injection contains bendamustine hydrochloride and uses the mixed solvent composed of the tertiary butanol and the injection water in the preparation process. The concentration of the bendamustine hydrochloride in the mixed solvents is 5-10 mg/ml. The volume ratio of the solvents is: 5-50% of tertiary butanol and the balance of injection water. The preparation process is that: measuring the tertiary butanol, adding injection water, mixing evenly, cooling to 2-15 DEG C, heat preserving, then adding the bendamustine hydrochloride, stirring to dissolve, filtering, filling, plugging, disking, freeze-drying, pressing the plug, out box, tying and packing.
US20110034549 Antitumoral Compounds A compound of general formula (I) wherein A, Y, W, R1, R2, R3, R4, R5, and R6 take various meanings for use in the treatment of cancer.
US20120016037 Method for prevention and treatment of Alzheimers Elderly individuals are administered dosages of Trans-resveratrol totaling between about 250 mg and 1 gram per day. Typically about 500 mg of Trans-resveratrol are orally administered to such individuals on a daily basis. As a result of the chemical action of Trans-resveratrol in the bodies of the subjects, Alzheimer's disease is prevented, or if already present, advancement is retarded and the existing mentally debilitating conditions of Alzheimer's disease are treated. A subject receiving the Trans-resveratrol experiences a reduction or illumination of the effects of Alzheimer's disease.
US20130039989 Pharmaceutical compositions comprising n-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide Disclosed are salts and crystalline forms of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide and salts thereof. Also disclosed are at least one pharmaceutical composition comprising at least one crystalline form of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide, at least one method of using at least one crystalline form of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide to treat cancer and/or other proliferative diseases, and processes to prepare crystalline forms of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide and salts thereof.
CN103623442A Household cleaning and sterilizing machine The invention provides a household cleaning and sterilizing machine. Acidic water with a high potential, strong oxidizability and a pH value of 2.0 to 3.5 can be produced through electrolysis of a saline solution. The acidic water with strong oxidizability is prepared by placing tap water containing salt in an electrolytic tank in which a positive electrode plate and a negative electrode plate are arranged and are separated by a cation exchange membrane and electrolyzing the water with high voltage current. Highly acidic water is produced after an oxidation reaction of a positive electrode and can be used for sterilization; and highly alkaline water is produced after a reduction reaction of a negative electrode. The strong-oxidizability water is nontoxic, tasteless and residue-free and especially applicable to sterilization of tableware, vegetable and fruit.
CN102952144A Crystal forms of asenapine maleate, and preparation method and medical composition thereof The invention discloses crystal forms of asenapine maleate, and a preparation method and medical composition thereof. The crystal forms A and B of asenapine maleate are stable in crystal form and high in micronization performance, and have a favorable dissolution rate in a water system after being subjected to micronization. Thus, the crystal forms are suitable for being prepared with the conventional medical auxiliary materials into the medical composition, and can be used for preparing an oral solid preparation having a fine dissolution rate.
WO2005087269A1 Method of inhibiting tumor proliferation It is intended to provide a method of inhibiting tumor proliferation which comprises the step of inhibiting the expression of PDGF-A or the binding of PDGF-A homodimer to PDGFRα. Activation of the PDGFR α-p70S6K signal transfer pathway by PDGF-AA, which is an important factor in tumor angiogenesis, relates to the prognosis of a patient suffering from tumor. By inhibiting the expression of PDGF-A in a tumor or a tissue around it or by inhibiting the binding of PDGF-A homodimer to PDGFRα, angiogenesis in the tumor and retention of the blood vessels can be inhibited and thus the tumor proliferation can be inhibited.
CN103550138A Sorafenib organogel and preparation method thereof The invention provides a sorafenib organogel and preparation method thereof. The sorafenib organogel is composed of an organic gelatinizing agent, an organic solvent, a dispersion stabilizer and an active medicine, wherein the organogel is a thermosensitive organogel with the gelatinizing temperature of 40-50 DEG C, the organogel is in a solution state at a high temperature and in a gel state after being cooled, and can be fast dispersed into a nanometer solution in the presence of water. The organogel disclosed by the invention is capable of obviously improving the in vitro dissolution rate of the sorafenib and the bioavailability of rat oral administration; the gel disclosed by the invention has the characteristics of being less in dosage of the gelatinizing agent, good in security, simple in preparation method and wide in use, and can be processed into preparations in various administration routes so that the application prospect is good.
US7314638 Preparing method for controlled released type tablet tamsulosin HCL and the tablet thereof The present invention relates to a simple and effective method for preparing a tamsulosin HCl sustained-release tablet and a tamsulosin HCl sustained-release tablet produced thereby. The method comprises the steps of: dissolving tamsulosin HCl as an active ingredient in an organic solvent; dissolving the tamsulosin HCl solution in hydroxypropylmethylcellulose phthalate to prepare a binder solution; and kneading the binder solution with a hydroxypropylmethylcellulose phthalate/glyceryl dibehenate mixture as an excipient and allows tamsulosin HCl to be released at uniformly controlled amounts in a subtained-release manner in vivo by controlling drug release rate according to different pH environments in vivo, so that it shows improved bioavailability and minimized side effects.
US8110574 Derivatives of 4-aminopiperidine and their use as a medicament A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.
CN102100409A Cigarette filtering agent for reducing tar, relieving cough and soothing throat The invention discloses a cigarette filtering agent for reducing tar, relieving cough and soothing throat, which is characterized by comprising the following raw material components by weight: 20 to 30 grams of meerschaum, 2 to 3 grams of American ginseng and 8 to 12 grams of spreading hedyotis herb, wherein the meerschaum is an adsorbent, adsorbs the tar and other intensely-poisonous and harmfulcarcinogenic substances in smoke effectively and protects the health of smokers; the American ginseng can refresh and enhance immunity; and the spreading hedyotis herb has an anticancer effect.
US20120095078 Methods of diagnosis and treatment of melanoma Methods for the diagnosis or prognosis of melanoma by detecting expression of ATF2 and MITF in melanocytes are provided herein. Also provided are methods of treating a melanocyte proliferative disorder with agents that modulate the transcriptional activity of ATF2 and/or MITF activity.
CN102351911A Method for synthesizing anticancer compound Na4Bi2Mn2W20C6H84N4O105 The invention provides a method for synthesizing an anticancer compound Na4Bi2Mn2W20C6H84N4O105, which relates to a method for synthesizing an anticancer compound. The method comprises the following steps: 1, dissolving Na2WO4 under magnetic stirring in deionized water and heating, then regulating pH to obtain a solution A; 2, simultaneously adding MnCl2, solid imidazole and Bi(NO3)3 dissolved inHCl, uniformly mixing and heating to react, then cooling to the room temperature, filtering and standing. The synthesized Na4Bi2Mn2W20C6H84N4O105 is a polyoxometallate modified by active imidazole, has strong inhibition effect on tumor cells of human stomach, and has good inhibition rate on tumor cells of liver cancer and colorectal carcinoma.
US7816521 1,2,4-benzotriazine-1,4-dioxides The compound 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide and pharmacologically acceptable salts thereof. A method of treating cancer in a subject is also described in which 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof is administered to tumor cells in a hypoxic environment. Also described is a method of radiosensitising in a subject tumor cells of solid tumors in hypoxic conditions by administering to the subject a pharmaceutical composition containing 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof in an amount sufficient to produce radiosensitivity in the tumor cells, and subjecting the tumor cells to radiation. A pharmaceutical composition is additionally provided containing a therapeutically effective amount of 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof and a pharmaceutically acceptable excipient, adjuvant, carrier, buffer or stabiliser.
CN102924567A Peptide compound and preparation method and use of peptide compound The invention discloses a novel peptide compound shown as a formula (I), pharmaceutically acceptable salts, pharmaceutically acceptable solvates, derivatives, isomers, crystal forms and pharmaceutically acceptable pro-drugs of the peptide compound. The invention also discloses a preparation method of the compound shown as the formula (I). The invention further discloses application of the peptide compound in preparation of drugs for treating and preventing thrombin mediated diseases and diseases related to thrombin.
EP1272907B1 Compliance tracking method There is provided a method for automatically tracking compliance in a manufacturing process involving successive manufacturing operations comprising selecting an object; associating an identifier with said object, said identifier comprising a memory; performing a first manufacturing operation relating to the object; following the successful completion of said first manufacturing operation, writing an associated compliance data item to the memory; performing one or more further manufacturing operations relating to the object; and following the successful completion of each said further manufacturing operation or any package thereof, writing an associated compliance data item to the memory.
CN103127026A Omeprazole enteric capsule and prepared method thereof The invention provides an omeprazole enteric capsule and a prepared method thereof and belongs to the field of medicinal preparation. The omeprazole enteric capsule can solve the problem that an existing omeprazole enteric capsule cannot be fully and timely released and is poor in stability after being taken orally. The omeprazole enteric capsule is composed of a pill core, an alkali layer, an isolating layer, an enteric layer and an outer layer from inside to outside in sequence. By means of the addition of the alkali layer, formula of each layer is optimized and full and timely release and stability of the omeprazole enteric capsule are guaranteed.
WO2007119006A1 New medicines for treatments against retroviruses This invention relates to the use of a sulphated or phosphated polysaccharide for the preparation of a medicine for treatments against retroviruses, more particularly against lentiviruses and oncoviruses, and particularly against HIV, including strains of these retroviruses that are resistant to known anti-retroviral agents; this medicine acts on the replication cycle of said retroviruses by inhibition of their RT.
EP2590938A1 Novel sulfonamide compounds for inhibition of metastatic tumor growth Therapeutic ureido-sulfonamide compositions having compounds with the formula R-Q-Ar-SO2NH2 are disclosed, which compounds selectively inhibit CAIX and CAXII, and which are effective to inhibit hypoxic tumor growth, suppress metastases, and impair and deplete cancer stem cells in mammals.
US20120270932 Personal Care Compositions with Improved Hyposensitivity The present invention provides personal care compositions comprising a carrier and a mixture of essential oil components having specific levels of eucalyptol, terpene materials and auxiliary fragrance materials. The compositions herein gentle to skin and have a fragrance and activity similar if the composition were made using the pure extracted essential oil.
CN1602847A Bupicomide hydrochloride drop pills and its preparation method The invention uses super micro shattering and buphenine drop pills producing the technology to produce fenfluramine drop pills, reaching the purposes such as increasing speed, and dissolution of disintegration, increasing the medicine stability, reducing the dose of auxiliary materials and decreasing cost, with rapid effect and convenient use. It can be buccal as well as deglutition, has remarkable conformity, and is especially suitable for children, older man, sicker in bed or with difficulty of swallowing.
CN101375843A Compound tranilast orally disintegrating tablet formulation and preparation method thereof The invention aims to provide a compound oral disintegrating tablet preparation which is composed of tranilast and salbutamol sulfate, and a preparation method thereof. The adopted specific technical proposal for achieving the purpose of the invention is as follows: the compound tranilast oral disintegrating tablet preparation is characterized in that the formula of the preparation is composed of the following components by parts by weight (by 1000 tablets): 80.0g of tranilast, 2.4g of salbutamol sulfate, 5-30g of disintegrant, 10-80g of filling agent, 5-25g of effervescing agent, 0.5-20g of flavoring agent and 0.3-3g of lubricant. The compound oral disintegrating tablet preparation which is prepared by the method can solve the shortcomings of the two drugs on the pharmacological effects during the treatment process of bronchial asthma and allow the compound oral disintegrating tablet preparation to relieve the asthma instantly and maintain and consolidate the effect; furthermore, the compound oral disintegrating tablet preparation has convenient administration, rapid onset of action, high bioavailability and good taste. The preparation method of the preparation has simple steps and low cost.
CN101723956A Crystal transformation process of (3,5-bis-trifluoromethyl)-6-amino-4H-(1,2) dithiol (4,3-b) pyrrole-5-ketone The invention discloses a crystal transformation process of (3,5-bis-trifluoromethyl)-6-amino-4H-(1,2) dithiol (4,3-b) pyrrole-5-ketone, which adopts nonpolar solvents of saturated fat alkane and aromatic hydrocarbon, and the like to treat the flocculent (3,5-bis-trifluoromethyl)-6-amino-4H-(1,2) disulfide bond (4,3-b) pyrrole-5-ketone and enables the crystal form to be transformed into amorphous or acicular crystal from flocculent crystal by heating. The transformation process has mild condition and simple operation; and the powder amorphous or acicular crystal compound prepared by the transformation process has good dispersibility, can improve the absorption and metabolism velocity of a medicine in the human body and provide the condition of preparing new dosage form for the medicine.
CN101049293A Medication composition of acetyl cysteine or its pharmaceutical salt and asarin A medical composition used to prepare the medicines for treating pneumonia, bronchial asthma, chronic obstructive pneumonia, and acute inflammation of lung is composed of acetylcysteine or its pharmacologically acceptable salt (20-1200 Wt. portions) and asarone (1-200). Its preparing process is also disclosed.
US7166625 Method for treating fibrotic diseases and other indications Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I:
EP2436390A1 Topical Anesthetic Uses of Szeto-Schiller Peptides Topical anesthetic compositions include Szeto-Schiller peptides and a dermatologically acceptable carrier, and optionally a vasoconstrictor and tyrosine. A method of providing local analgesia to the skin involves applying to skin the topical anesthetic compositions.
US20080213295 Estrogen receptor polypeptide which induces immune respone; for use in treatment and prevention of cell proliferative disorders; antitumor agents The present invention is generally directed to HER-2/neu fusion proteins, nucleic acid molecules encoding HER-2/neu fusion proteins, viral vectors expressing HER-2/neu fusion proteins, and pharmaceutical compositions (e.g., vaccines) comprising the HER-2/neu fusion proteins and/or nucleic acid molecules encoding the HER-2/neu fusion proteins. The present invention is also directed to methods of treating or preventing cancer by eliciting or enhancing an immune response to the HER-2/neu protein, including for uses in the treatment of malignancies associated with the HER-2/neu oncogene.
CN101143139A Stable tiopronin injection and preparation method thereof The invention relates to a preparation method of an injection and concretely relates to a stable tiopronin injection and the preparation method of the stable tiopronin injection. The stable tiopronin injection contains the effective dosages of the tiopronin, water for injecting and an aminophenol antioxidant, wherein the weight concentration of the aminophenol antioxidant is 0.1 to 0.64 percent. The invention conquers the prior technical problem of the bad stability of the tiopronin in the water; the injection of the invention has the advantage of high stability and can always keep good stability during the period of storing, transporting and using; compared with the prior freeze-dry powder injection, the injection of the invention presents better stability when medicating the vein.
CN103006591A Pamicogrel dispersible tablets and preparation method thereof The invention relates to pamicogrel dispersible tablets and a preparation method thereof, and belongs to the technical field of western medicinal preparations. 1000 dispersible tablets comprise the following components: 80 grams of pamicogrel, 50 grams of mannitol, 30 grams of starch, 30 grams of microcrystalline cellulose, 10 grams of cross-linked sodium carboxymethyl cellulose, 4 grams of silicon dioxide, 2 grams of magnesium stearate, 0.3 gram of lauryl sodium sulfate, and 75 milliliters of 1 percent aqueous solution of hydroxypropyl methylcellulose. The curative effect of the pamicogrel preparation is improved, the side effect on a human body is reduced, and the dispersible tablets can be quickly disintegrated to form uniform suspension when being put into water and have the characteristics of convenience in administration and high bioavailability. The preparation method for the dispersible tablets is simple and low in cost, and does not require special production equipment.
US20080045598 aromatase inhibitors such as N-methyl-N-[2-(4'-nitro benzyloxy)-4-nitrophenyl] methanesulfonamide, used for suppressing aromatase activity expression in breast cancer cells; anticarcinogenic agents Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I: wherein R1 may be alkyl, cycloalkyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; R2 is H, alkyl, aryl, alkylaryl, arylalkyl, and cycloalkyl; R3, with the base nitrogen, forms an amide or sulfonamide; R4 is selected from nitro, amine, amide, and benzamide; or a pharmaceutically acceptable salts thereof Also provided are small molecule selective aromatase inhibitors having a molecular weight of less 500 g/mol. In some embodiments, the small molecule selective aromatase inhibitors described herein have a molecular weight of less than 450 g/mol. Also provided are methods for suppressing aromatase activity expression in cancer cells comprising the step of administering a pharmaceutically effective amount of a small molecule aromatase inhibitor to a subject in need of such treatment. In one embodiment, the cancer cells are breast cancer cells.
CN103554070A Ascorbic acid bismuth oxide, preparation method and application of ascorbic acid bismuth oxide The invention relates to a new substance of ascorbic acid bismuth oxide, a preparation method and the application of the ascorbic acid bismuth oxide. The preparation method is characterized by comprising the following steps: (1) weighing and inputting raw materials of bismuth hydroxide, ascorbic acid and water into a reaction kettle, wherein the bismuth hydroxide and the ascorbic acid are in the substance amount ratio of 1:1; (2) starting a machine for performing chemical reaction for half a hour; (3) stopping the machine for half a hour, and discharging the reaction product ascorbic acid bismuth oxide. The ascorbic acid bismuth oxide prepared by the preparation method can be applied to the field of medicine and food, for example, the ascorbic acid bismuth oxide can serve as a stomachic digestion Vc (vitamin C)-supplement antioxidant preservative, a stomachic digestion VC-supplement food additive, and a medicament for treating stomach illness, stomach cancer, bronchitis, pneumonia, hepatitis, liver cancer and hypertension.
WO2008061308A1 Protein tyrosine phosphatase modulators The present invention relates to protein tyrosine phosphatase (PTP) modulators, in particular PTP inhibitors and their use in the treatment or prophylaxis of disorders modulated by PTP such as cellular proliferation disorders; autoimmune diseases for example diabetes or inflammatory diseases; infections caused by viruses using PTPases for infectivity; angiogenesis mediated disorders; bone disorders; and vascular tone, vascular permeability or VEGF mediated disorders.
WO2009151090A1 Rapidly disintegrating preparation containing calcium carbonate Disclosed is a technique for producing a rapidly disintegrating preparation which contains calcium carbonate, can rapidly disintegrate with a small quantity of water or saliva in the oral cavity and has such tablet physical properties that can fully withstand the conditions for market distribution in a rotary compression molding machine without the need of employing any complicated process or any specialized production facility. Specifically disclosed is a rapidly disintegrating preparation containing calcium carbonate, which is shaped by the direct tableting of a material comprising at least the components (A) and (B) shown below in a compression molding machine, has a tablet hardness of 40 to 200 N, has a tablet wear rate of 1% or less, and requires 60 seconds or shorter for the disintegration in the oral cavity. (A) Calcium carbonate having a 50% particle diameter of 20 to 100 μm as measured on the powder particle size by a laser diffraction method. (B) A component which can increase the moldability of the whole preparation when mixed with calcium carbonate.
US20080214504 Vitamin B6 Related Compounds and Methods for Recovery From Trauma The present invention includes a method of promoting recovery from trauma in a patient in need thereof comprising administration of a therapeutically effective amount of a vitamin B6 related compound (excluding vitamin B6), preferable compounds include pyridoxal-5′-phosphate, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxy-4,5-animal, and pyridoxine phosphate analogues.
US20090274675 Migraine tonic This invention is proposing a combination of a system of migraine headache remedies from non-prescription pharmaceuticals in the form of an aqueous drinkable tonic utilizing as the component foundation the main ingredient Ubiquinone (Co-enzyme-Q10) coupled with one or more of the following non-prescription natural or synthesized pharmaceuticals to include but are not inclusive of Tanacetum Parthenium, or Hypericin and/or Hyperforin, Petasin, Magnesium Citrate, and Riboflavin, the selection of which is determined upon the user and the user's other medications.
US20070238649 Agents for Regulating Adiponectin Receptor Expression The present inventors revealed by using fasted and refed mice, that AdipoR1/R2 is a regulator of metabolic sensitivity to nutritional conditions and insulin. They showed that mRNA level of AdipoR1/R2 increased by STZ treatment, and that this increase was restored by insulin. The present inventors confirmed in vitro that insulin reduces AdipoR1/R2 mRNAs in myocytes and such. It was also confirmed that in insulin-resistant models, the AdipoR1/R2 expression was downregulated, and that AMP kinase activation by adiponectin was decreased. The present inventors discovered by using insulin signaling pathway inhibitors, that the downregulation of adiponectin receptors by insulin was mediated by the PI3-kinase/Foxo1 pathway.
US20080199443 Bone Morphogenetic Variants, Compositions and Methods of Treatment Human cartilage-derived morphogenetic protein variant polypeptides and isolated nucleic acids are provided. Also provided are vectors, host cells, and recombinant methods for producing human cartilage-derived morphogenetic protein variants polypeptides. Therapeutic methods useful for treating musculoskeletal disorders and joint repair with such variants are also provided.
WO2013047923A1 Nanoemulsion containing a polyaspartic acid derivative and personal care composition containing same The present invention relates to a nanoemulsion comprising 1-20 parts by weight of polyaspartic acid derivative, 1-5 parts by weight of saturated lecithin, 1-10 parts by weight of dissolution aid, 0.1-5 parts by weight of rhizonlecithin, and 1-5 parts by weight of sucrose fatty acid ester, and also relates to a personal care composition containing said nanoemulsion. The personal care composition containing the nanoemulsion of the present invention can induce biosynthesis of collagen, and has very good inhibitory effects against MMP-1 (matrix metalloproteinase-1) and has anti-allergic effects.
WO2011121109A1 Methods and compositions comprising ampk activator (metformin/troglitazone) for the treatment of myotonic dystrophy type 1 (dm1) The present invention relates to methods and compositions for the treatment of Myotonic Dystrophy type 1 (DM1) with an AMPK activator .
WO2008032506A1 Mineral water and process for producing the mineral water Mineral water which contains mineral ingredients released from a soft porous ancient marine humic substance and including a calcium ingredient, the calcium ingredient accounting for at least 90% of the mineral ingredients. The mineral water contains SiO2, Al, Fe, Ca, Mg, K, Ti, P, Na, and Mn which are mineral ingredients released from a soft porous ancient marine humic substance and in which the calcium ingredient accounts for 90 wt.% or more of the total amount of the mineral ingredients. Also provided is a process for mineral water production which comprises passing raw water through superposed layers of a soft porous ancient marine humic substance ceramic obtained by adhering a powder of a soft porous ancient marine humic substance in a layer arrangement to a particulate ore of a soft porous ancient marine humic substance and burning them and through superposed layers comprising a burned powder of a soft porous ancient marine humic substance to dissolve mineral ingredients, i.e., SiO2, Al, Fe, Ca, Mg, K, Ti, P, Na, Mn, Co, Ba, Zn, Sn, V, Ni, and Cu, in the raw water. Thus, mineral water containing the calcium ingredient in an amount of 90 wt.% or larger based on the total amount of the mineral ingredients is produced.
CN103446430A Pharmaceutical composition for preventing birth defects and improving memory The invention relates to a pharmaceutical composition for preventing birth defects and improving memory, which comprises ophiopogon root, wolfberry fruit, prepared fleece-flower root, epimedium, dodder, glossy privet fruit, radix rehmanniae preparata, rhizoma atractylodis macrocephalae, vitamin A, beta-carotin, vitamin complex B, vitamin C, vitamin D, vitamin E, vitamin K, macroelements (calcium, potassium and magnesium) and microelements (zinc, selenium, iron, chrome, copper, molybdenum, iodine, manganese, germanium, silicon and strontium). The pharmaceutical composition is mainly suitable for women before pregnancy, pregnant women and wet nurses, is very effective in preventing birth defects and improving memory, has the effects of health care and invigoration, and can not generate any side effect after long-term application.
WO2004098591A3 Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases The present invention relates to compounds that act as inhibitors of QC including those represented by the general formulae ( 1 to 9): and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleepwakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
US20050009845 Thienopyrimidine compounds as protein tyrosine kinase inhibitors The present invention relates to thienopyrmidine compounds of formula (I) (one of A1 and A2 is S and the other is CH), salts thereof, as well as use and preparation of the same. These compounds are inhibitors of various protein tyrosine kinases (PTKs) of the ErbB family and consequently are useful in the treatment of disorders mediated by aberrant activity of such kinases.
EP1773813A1 Crystalline polymorph of pipindoxifene hydrochloride monohydrate The present invention is directed to a crystalline polymorph of pipindoxifene hydrochloride monohydrate, compositions containing the same, preparations thereof, and uses thereof.
US20100140131 Production of an Oxaliplatin Mixture and a Container and a Container Set for Said Mixture The invention relates to a process for the preparation of an aqueous oxaliplatin solution in which oxaliplatin is dissolved in water by addition of an acid up to an oxaliplatin concentration greater than an acid-free aqueous oxaliplatin solution. The invention relates also to a container and a set of containers containing the solution.
EP1009846B1 Alphavirus-derived vectors useful as vaccines providing protection against paramyxovirus infection A vector comprising a first DNA sequence which is complementary to at least part of an alphavirus RNA genome and having the complement of complete alphavirus DNA genome replication regions, a second DNA sequence encoding a paramyxovirus protein, particularly a respiratory syncytial virus fusion (RSV F) protein or an RSV F protein fragment that generates antibodies that specifically react with RSV F protein, the first and second DNA sequences being under the transcriptional control of a promoter is described. Such vector may be used to produce an RNA transcript which may be used to immunize a host, including a human host, to protect the host aginst disease caused by paramyxovirus, particularly respiratory syncytial virus, by administration to the host. The RNA transcript may be formed by linearization of the vector through cleavage at a unique restriction site in a plasmid vector and then transcribing the linear molecule.
EP2570408A1 Hexaketide compound and medicinal use thereof The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof; to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent; and also to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, or preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
US20060068389 Methods and compositions for inhibiting hiv replication Pharmaceutial composition comprising compounds and/or compositions useful to inhibit HIV replication are disclosed. Methods of treating individuals infected with HIV are disclosed. Methods of preventing HIV infection in high-risk individuals are disclosed.
US20120295909 Alkyl-heterocycle carbamate derivatives, their preparation and their therapeutic application The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
WO2012046902A1 Method for treating parkinson's disease through the control of the vdac1 protein The present invention relates to a method for treating Parkinson's disease through the control of the voltage-dependent anion channel 1 (VDAC1) protein. In particular, the present invention relates to a pharmaceutical composition for treating Parkinson's disease including a VDAC1 protein controller. The VDAC1 protein controller comprises: a drug that inhibits the generation of the mRNA of VDAC1, a drug that inhibits mitochondrial permeability transition pore (MPTP), a mitochondrial calcium uptake inhibitor, etc. The present invention also relates to a method for treating Parkinson's disease comprising the step of dosing an individual with a VDAC1 protein controller. The present invention is expected to be capable of providing a method for fundamentally treating Parkinson's disease by preventing abnormal mitochondrial function and/or restoring same.
CN101973989B Thiazole amide compound and medicinal application thereof for treating malignancy The invention relates to a thiazole amide compound and the medicinal application thereof for treating malignancy. The thiazole amide compound is an ideal Bcr-Abl and Src protein tyrosine kinase inhibitor and has good effect on malignancy, such as chronic myelogenous leukemia, acute myelogenous leukemia, acute lymphoblastic leukemia, myelodysplastic syndromes, lung cancer, oophoroma, prostatic cancer, soft tissue sarcoma, glioblastoma, and the like, and meanwhile, the invention has the advantages of little dosage and few side effects.
US20110027171 Ph sensitive liposome composition Using liposomes to deliver bioactive agents to cancer or tumor cells and compositions of specific lipids that form liposomes to deliver a biologically active agent.
EP2072047A1 Therapeutic agent for opthalmic disease Use of (2R)-2-propyloctanoic acid, a salt thereof or a prodrug thereof for the manufacture of an agent for the prevention, treatment and/or inhibition of progression of an ophthalmic disease selected from the group consisting of glaucoma, cataract, retinal detachment, muscae volitantes, age-related macular degeneration, diabetic retinopathy, macular edema, myopia, asthenopia, dry eye, amaurosis fugax, choked disc, papillitis optica, retrobulbar neuritis, toxic amblyopia, optic atrophy, higher visual pathway lesion, internuclear ophthalmoplegia, gaze palsy and ischemic optic neuropathy, in which an amount per dose is from 0.3 ng to 500 mg.
US20060014735 immunoglobulins; affinity chromatography The present invention relates to an IgG-binding compound, which more specifically has affinity for human IgGs of κ-type and functional derivatives thereof. More specifically, the compound according to the invention comprises an N,N-alkylated urea moiety located between an aromatic part and another part, which is a linear or cyclic substituted or unsubstituted aliphatic group. The compound binds to a pocket-shaped binding site present on all human IgG κ-Fabs, which site is located between the two domains (CH1 and CL) of its constant part. Accordingly, the compound according to the invention is a ligand for human IgGs of κ-type, and consequently, the invention also relates to a separation matrix for affinity chromatography, which matrix comprises said compound, as well as to other uses of the compound.
WO2014041393A1 Combination of compounds derived from gallic acid for the treatment of cancer The invention relates to a combination of compounds derived from gallic acid, with an antitumoural and antimetastatic activity via a mechanism that involves the induction of apoptosis and the immunogenic death of the tumour cells and the subsequent activation of the specific immune response. The invention also relates to a composition containing a combination of derivatives of gallic acid and pharmaceutically acceptable excipients for the production of useful medicaments in the treatment of cancer. The invention further relates to the use of said composition as a coadjuvant in conventional chemotherapy, reducing the doses of chemotherapeutic agents used in the treatment of cancer.
CN1895393B Health-care composition for regulating blood fat A health-care composition for regulating blood fat and decreasing TC, TG and HDL is prepared from ganoderma extract, haw extract, perilla oil and phosphatide.
CN101272786A Lotion preparation containing pyridonecarboxylic acid derivative It is intended to provide a lotion preparation which exerts an excellent antibacterial effect, is excellent in the stability of active ingredient and does not contain an additive having a safety problem. The lotion preparation contains (a) 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid and/or a pharmaceutically acceptable salt thereof, (b) a lower alcohol, (c) a water-soluble polymer and (d) a polyhydric alcohol and the pH of the preparation is in the range of 9 to 12.
CN103356555A Application of Sarcaboside A in erythrocyte-increasing medicines The invention relates to new application of a compound Sarcaboside A in the field of pharmacy, particularly application of Sarcaboside A in preparing erythrocyte-increasing medicines. The application of Sarcaboside A in preparing medicines for treating low erythrocyte is disclosed for the first time. Since the framework type is brand-new and has unexpectedly high activity for inhibiting low erythrocyte, the Sarcaboside A does not has the possibility of any inspiration given by other compounds, has outstanding substantive characteristics, and obviously has significant progress in preventing and treating low erythrocyte.
CN103751705A Eye drops for treating vitreous opacity and preparation method thereof The invention discloses eye drops for treating vitreous opacity and preparation method thereof. The eye drops are prepared from the following raw materials in parts by weight: 80-120 parts of bovine eyeballs, 10-15 parts of cassia seed, 15-20 parts of turmeric, 12-16 parts of radix scrophulariae, 9-13 parts of cortex trichosanthis, 10-15 parts of radix ophiopogonis, 5-10 parts of prepared rehmannia, 16-22 parts of notoginseng bud, 10-15 parts of radix curcumae, 8-12 parts of mulberry leaf, 14-18 parts of ash bark, 5-10 parts of palmleaf raspberry root, 10-15 parts of butterflybush flower, 7-14 parts of buerger pipewort flower, 11-17 parts of scutellaria baicalensis, 15-20 parts of chrysanthemum leaf, 10-15 parts of rhizoma acori graminei, 5-10 parts of schisandra chinensis, 10-15 parts of caltrop, 0.1-0.3 parts of borax, 0.3-0.5 part of sodium hyaluronate, and 0.4-0.8 part of sodium chloride. The eye drops are compatible in raw materials to achieve the effects of clearing heat and cooling blood, activating blood and diminishing edema, nourishing yin and moistening dampness, removing stasis and eliminating turbidity, and removing nebula, can be used for remarkably improving eye blood circulation, improving eye cell activity, and improving and relieving the symptom of vitreous opacity, have the characteristics of good curative effect, high cure rate, no adverse response and high safety, and is worthy of clinical application and popularization.
US20120129872 Fused heteroaryl inhibitors of pro-matrix metalloproteinase activation This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
EP1954297A1 Use of xenon for organ protection Use of xenon is described. Xenon is used as an organ and/or tissue and/or cell protectant in the manufacture of a pharmaceutical for the protection from injury of organs and/or tissue and/or cells that express HIF.
CN101972225A Pirfenidone-contained gel composition The invention provides a pirfenidone-contained gel composition and a preparation method thereof. The pirfenidone-contained gel composition comprises pirfenidone and other pharmaceutically acceptable accessories. The invention further illuminates the clinical use method and the applications of the preparation mode.
WO2012057599A1 Anti-mycobacterial agents The invention relates to novel compounds which act has anti-mycobacterial properties, in particular anti-tuberculosis. The novel molecules of AM1, AM2, AM3, AM4, AM5, AM6, AM7, AM8, AM9, AM10, AM11, AM12, AM13, AM14, AM15, AS1, AS2, AS3, AS4, AS5, AS6, AS7, AS8, AS9, AS10, AS11, AS12, AS13 and AS14 are of substituted Mannich base and Schiff base which contains anti-tuberculosis properties. The invention presents the method for preparation of compounds AM1, AM2, AM3, AM4, AM5, AM6, AM7, AM8, AM9, AM10, AM11, AM12, AM13, AM14 and AM15, wherein the steps includes: (a) s synthesizing an aromatic ester derivative using an aromatic carboxylic acid and alcohol in the presence of concentrated sulfuric acid; (b) synthesizing an acid hydrazide derivative using the aromatic ester derivative from step (a); (c) synthesizing Schiff bases using the acid hydrazide derivative from step (b); and (d) synthesizing Mannich bases using the Schiff bases from step (c). The present invention presents the method for preparation of compounds AS1, AS2, AS3, AS4, AS5, AS6, AS7, AS8, AS9, AS10, AS11, AS12, AS13 and AS14, wherein the steps includes: (a) synthesizing an aromatic ester derivative using an aromatic carboxylic acid and alcohol in the presence of concentrated sulfuric acid; (b) synthesizing an acid hydrazide derivative using the aromatic ester derivative from step (a);and (c) synthesizing Mannich bases using the Schiff bases from step (b).
WO2014068988A1 Pyrazolopyridine derivatives as ttx-s blockers The present invention relates to pyrazolopyridine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
CN101904845A Amlodipine nicotinate with synergetic pressure reducing function and treatment composition thereof with statin drugs The invention relates to application of common amlodipine nicotinate capable of improving the blood pressure reduction effect of amlodipine and a preparation method, wherein the common amlodipine nicotinate can be independently applied or can be mixed with statin lipid-reducing drugs or pharmaceutical salts thereof. The composition can be used for treating patients (including human beings) suffered from angina, atherosclerosis, and/or patients combing the high blood pressure with hyperlipemia and patients with dangerous heat symptoms and improving the pharmacologic efficiency of the traditional like medicines.
US20090069440 Deuterium-enriched atomoxetine The present application describes deuterium-enriched atomoxetine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
EP2177517A1 Amino substituted 2-(2,6-dioxopiperidin-3-yl)-phthalimide for reducing TNF alpha levels Substituted 2-(2,6-dioxopiperidin-3-yl)phtalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines reduce the levels of TNFα in a mammal. Typical embodiments are 1-oxo-2(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafluoroisoindoline and 1,3-dioxo-2-(2,6-dioxo-3-methylpiperidin-3-y1)-A-aminoisoindoline.
US20100291174 Biologically active device and method for its production The present invention is directed to a biologically active device with a main body made from a polymer, in which bioactive nanoparticles of one or several materials are embedded, wherein the nanoparticles of at least one material proliferatively act on a biological material contacted by the device, and wherein nanoparticles of a different material act in an anti-proliferative manner on biological material in the ambience of the device. The invention is also directed to a method of manufacturing a biologically active device with a main body made from a polymer, wherein nanoparticles of several different materials are dispersed in an injection-moldable fluid, and the fluid is shaped into the polymer main body by means of injection molding and curing, such that the nanoparticles are dispersed in the bulk of the polymer main body. According to the invention, the nanoparticles are generated by arranging at least two substrates of different material in a vessel filled with a fluid material, and by generating the nanoparticles by abrasion from the surface of the substrates in the fluid with laser radiation.
CN102442985A Natural compound P71 with activity of inhibition of tumor cell reproduction and growth, and application thereof The present invention discloses a natural compound P71 with an activity of inhibition of tumor cell reproduction and growth, and an application thereof. The structural formula of the natural compound P71 is represented by the formula I. The natural compound P71 or the pharmaceutically-acceptable salts of the natural compound P71can be used for preparation of drugs for inhibition of eukaryote tumor cell reproduction, and drugs for prevention and/or treatment of tumors. In vitro anti-tumor test results show that: the compound P71 provides good inhibition effects for breast cancer cells (MCF-7), lung cancer cells (A549), ovarian cancer cells (SKOV3), colon cancer cells (Caco2, SW480) and African green monkey kidney fibroblasts (COS-7). (formula I)
WO2014049366A1 Treatment of wolfram syndrome-related neurodegeneration Provided is a method of treating and/or preventing Wolfram Syndrome (WS)-related neurodegeneration (i.e. of Wolfram Syndrome-Associated Neuronal Degeneration), by increasing the expression and/or functional activity of p21. A method of screening for pharmacological agents useful in treating and/or preventing such conditions is also provided.
CN102232941A Antrodia camphorata cyclohexenone compound for inhibiting ovarian cancer tumor cell growth The invention relates to a new application of a compound. 4-hydroxy-2,3-dimethoxy-6-methy-5(3,7,11-trimethyl-dodeca-2,6,10-trienyl)-cyclohex-2-enone is separated and purified from antrodia camphorata extract. The cyclohexenone compound can be applied to inhibition of ovarian cancer tumor cell growth, and also can be applied to medicinal compositions for inhibiting ovarian cancer tumor cell growth.
US20100184803 Treatment of Lysosomal Storage Diseases Methods and compositions useful in the treatment or prevention of lysosomal storage diseases, such as Pompe's disease, Fabry's disease, Gaucher's disease, and Niemann-Pick disease, are provided. The treatment includes administering to a subject a farnesyl transferase inhibitor compound. The treatment may also include enzyme replacement therapy or gene therapy.
CN103191086A Application of aspidin BB in dryopteris fragrans in preparing antitumor medicines The invention relates to an application of aspidin BB in dryopteris fragrans in preparing antitumor medicines. According to the invention, through in-vitro MTT method, in-vivo nude mice experiments, and nuclear magnetic resonance detections, it is proved that aspidin BB has good activity against various tumor cells and especially MCF-7 tumor cells. When aspidin BB is added into different excipients, the mixtures can be processed into any pharmaceutically acceptable preparation. Aspidin BB in dryopteris fragrans is safe and reliable, and has the characteristics of low toxic and side effect, clear treatment effect, and the like. Dryopteris fragrans has the advantages of rich resource, convenient collection, simple extraction process, and suitability for industrialized productions.
US20080234291 Apolipo-protein B (apoB) secretion and microsomal triglyceride transfer protein (MTP) inhibiting properties; hyperlipidemia, obesity, or type II diabetes; solubility, taste modifying agent and an antioxidant The present invention concerns an oral solution comprising the MTP inhibitor mitratapide or an pharmaceutically acceptable acid addition salt thereof, a process for preparing such solutions, and their use in the treatment of MTP-related disorders such as hyperlipidemia, obesity, or type II diabetes.
WO2006064826A1 MEDICINAL COMPOSITION CONTAINING FBPase INHIBITOR Means for the treatment of diabetes which has the high ability to reduce the blood sugar level and is effective in alleviating pancreatic β-cell dysfunction. It is a medicine comprising a combination of an FBPase inhibitor and an insulin resistance reducer which is 5-[4-(6-methoxy-1-methyl-1H-benzoimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione or a pharmacologically acceptable salt thereof.
CN103720693A Application of five normal bases of human body in preparation of medicines for cancer treatment The invention discloses application of five normal bases of human body in preparation of medicines for cancer treatment. The five bases are applicable to cancer treatment field, and are prepared into an oral preparation, an injection, a slow-release preparation or a targeting preparation. Standard anti-tumor effect control proves that the five normal bases participating in human metabolism, when achieving a certain concentration in vivo and in vitro, have effects of inducing tumor cell apoptosis and resisting tumor angiogenesis in different degrees. The application disclosed by the invention has the advantages that the five bases, compared to other anti-tumor medicines, have broad-spectrum and low-toxicity anti-tumor effect, and are applicable to chemical treatment of malignant tumors such as gastric cancer, lung cancer, liver cancer, colon cancer, breast cancer, tumors of reproductive system and the like with obvious anti-tumor effect; the five normal bases, in conventional dosage, are free from bone marrow suppression and important organ injury, and are better in anti-tumor effect compared to normal nucleoside.
CN101234144A Dropping pills for treating toothache and preparation thereof The invention relates to a dropping pill for treating toothache and a preparation method thereof, wherein the dropping pill is composed of piper longum L., clove and borneol according to a weight proportion of 10-100 : 1-80 : 1-50. The dropping pill for treating toothache provided by the invention has analgesic and detumescent action and inflammation and pain relieving effect, which is suitable for the symptoms of wind-fire toothache, painful gum and toothache resulted from periodontitis and pericoronitis and so on. The method adopts a solid dispersion technology and uses polyethylene glycol as a carrier, thus being able to greatly improve the dissolution rate of the medicine and being helpful for the medicine adsorption, which results in a higher bioavailability. At the same time, the dropping pill formulation is characterized in three smalls (small dosage, small volume and small toxic and side effect) and three efficiencies (high efficiency, quick efficiency and long term efficiency), which results in quick effect, easy administration and remarkable curative effect, thus being able to satisfy the requirement of the patients.
WO2013066208A3 Pharmaceutical composition based on epigallocatechin gallate-containing nano-micelles and use thereof The invention relates to the field of pharmaceuticals. The aim of the present invention is to produce nano-micellar structures containing EGCG and providing the technical result of improved peroral bioavailability. This aim is achieved by a novel pharmaceutical composition for peroral administration containing epigallocatechin-3-gallate as active ingredient and a special-purpose additive, said special-purpose additive being in the form of an oxyethylene-oxypropylene block copolymer having a hydrophobic block content of less than 50 mass% and a hydrophobic block molecular mass of 2250 daltons or more, wherein the mass ratio of active ingredient to block copolymer is 1:1 - 10:1. The compositions improve the absorption of the active compound in the bloodstream when said active compound is administered perorally.
WO2014072419A1 Novel anti-hiv compounds The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing fluorine on the Central ring. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show higher activity against NNRTI-resistant strains of HIV-1.
US6867306 Process for the synthesis of atorvastatin form v and phenylboronates as intermediate compounds The present invention discusses a novel process for the synthesis of [R-(R*,R*)]-2-(4-fluorophenyl)-B,D-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium, atorvastatin. The compound so prepared is useful as inhibitor of the HMG-CoA reductase and may thus be used as hypolipidemic and hypocholesterolemic agent.
US20080182803 extract from Cassia or Senna plants comprises rubrofusarin gentiobioside with egg white, egg membrane, milk whey, yeast/vegetable proteins, soy bean, L-cysteine, L-methionine, and vitamin C; synergistic; intracellular biosynthesis of glutathione stimulator; liver, brain, vision, or immune disorders There is provided an oral composition capable of stimulating intracellular biosynthesis of glutathione in order to maintain in-vivo (i.e., in tissues and cells) glutathione level at a high level, by adding an active ingredient other than an amino acid precursor from a viewpoint of increasing intracellular glutathione synthesis, as a method which is an alternative or can be combined with a method of supplying an amino acid precursor to be used in glutathione biosynthesis. The oral composition is used for maintaining or increasing intracellular glutathione level and contains at least one rubrofusarin glycoside in an amount that is effective for increasing the intracellular glutathione.
US20120165252 Method of Regulating Glucose Metabolism, and Reagents Related Thereto The present invention provides methods and compositions for modification and regulation of glucose and lipid metabolism, generally to reduce insulin resistance, hyperglycemia, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoproteinemia (such as chylomicrons, VLDL and LDL), and to regulate body fat and more generally lipid stores, and, more generally, for the improvement of metabolism disorders, especially those associated with diabetes, obesity and/or atherosclerosis.
CN103193642A Carvacrol derivatives and synthetic method and application thereof The present invention discloses a class of carvacrol derivatives capable of preventing cardiovascular diseases as shown in a structural formula (I). Relative to original medicines, the carvacrol derivatives have the characteristics of increasing lipid solubility, changing absorption performance, increasing stability, improving efficacy, and reducing toxic and side effects.
CN101889985B Medicament-carrying nano microspheres and preparation method thereof The invention relates to medicament-carrying nano microspheres. Each medicament-carrying nano microsphere comprises a core and a surface layer, wherein the core is made of a biologically degradable polymer material and a hydrophobic medicament; the surface layer is made of chitosan or derivative of the chitosan; in the core, the biologically degradable polymer material accounts for 50 to 95 weight percent and the hydrophobic medicament accounts for 5 to 50 weight percent; based on the weight of the core, the surface layer is 2 to 10 percent; and the particle size of the medicament-carrying nano microsphere ranges from 50 to 500 nanometers. The preparation method of the medicament-carrying nano microspheres of the invention comprises: slowing injecting organic solvent solution which contains a carrier material and the hydrophobic medicament in a large amount of water and adding aqueous solution of the chitosan or the derivative of the chitosan; or slowly injecting the organic solvent solution which contains a carrier material and the hydrophobic medicament in a large amount of the aqueous solution of the chitosan or the derivative of the chitosan to prepare the medicament-carrying nano microspheres. In the invention, the problem of preparing the medicament-carrying nano microspheres with stable hydrophilic surface layers by using the biologically degradable polymer or random copolymer is solved, and the drawbacks of use of an amphiphilic block (or graft) copolymer which is difficult to synthesize and easily falling of the hydrophilic surface layers of the prior art are overcome.
US20090163532 Aqueous Gel Formulations Containing Immune Response Modifiers Aqueous gel formulations, including an immune response modifier (IRM), such as those chosen from imidazoquinoline amines, tetrahydroimidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, 1,2-bridged imidazoquinoline amines, imidazonaphthyridine amines, imidazotetrahydronaphthyridine amines, oxazoloquinoline amines, thiazoloquinoline amines, oxazolopyridine amines, thiazolopyridine amines, oxazolonaphthyridine amines, thiazolonaphthyridine amines, pyrazolopyridine amines, pyrazoloquinoline amines, tetrahydropyrazoloquinoline amines, pyrazolonaphthyridine amines, tetrahydropyrazolonaphthyridine amines, and 1H-imidazo dimers fused to pyridine amines, quinoline amines, tetrahydroquinoline amines, naphthyridine amines, or tetrahydronaphthyridine amines, are provided. Methods of use and kits are also provided.
CN102151282A Application of iridoid glycoside and derivatives thereof as plasmin inhibitor and medicine composites of plasmin inhibitor The invention relates to application of iridoid glycoside and derivatives thereof as plasmin inhibitor and medicine composites of plasmin inhibitor belonging to the technical field of natural medicine extractives. The iridoid glycoside and derivatives thereof are geniposide, loganin or pharmaceutically acceptable salt or ester forms.
CN103550238A Composition containing procyanidine The invention discloses a composition containing procyanidine. The composition is prepared by adopting procyanidine and geniposide as main raw materials. The composition has an exact therapeutic effect on chemical liver injury and has characteristics of instant effectiveness, short treatment course, low cost, small side effect and the like.
EP0986561B1 Compounds for inhibition of ceramide-mediated signal transduction Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with TNF-α and fibroblast proliferation in vivo and in vitro. The compounds of the invention neither appreciably inhibit the activity of cAMP phosphodiesterase nor the hydrolysis of phosphatidic acid, and are neither cytotoxic nor cytostatic. Preferred compounds of the invention are esters. Methods for the use of the novel compounds to inhibit ceramide-mediated intracellular responses in stimuli in vivo (particularly TN-α) are also described. The methods are expected to be of use in reducing inflammatory responses (for example, after angioplasty), in limiting fibrosis (for example, of the liver in cirrhosis), in inhibiting cell senescence, cell apoptosis and UV induced cutaneous immune suppression. Compounds having enhanced water solubility are also described.
CN102580104A Narcotic drug composition for examining or curing cavities and preparation method of narcotic drug The invention discloses a narcotic drug composition. Per 100g of the narcotic drug composition contains 2g of lidocaine hydrochloride and 0.5-2g of sodium hyaluronate. Compared with existing anesthetics for examining and curing the cavities, a lidocaine hydrochloride topical gel uses the sodium hyaluronate with a good histocompatibility as a tackifier, and after the narcotic drug composition is used, residues are easy to absorb and decompose by human bodies. Simultaneously, when used in gynaecology cavities, the narcotic drug composition is capable of effectively relieving wound pains, promoting wound healing, alleviating inflammation, and preventing adhesion, and the narcotic drug composition has a wide application prospect.
EP1704870A1 Use of iron compounds as radiosensitizers There is provided a radiosensitizer containing an iron compound, more specifically, a radiosensitizer containing an iron compound selected from an inorganoiron compound, such as iron chloride, iron oxide, iron hydroxide, and iron sulfate; and an organoiron compound, such as saccharated ferric oxide, iron citrate, iron gluconate, chondroitin sulfate/iron colloid, cideferron, ferrotrenine, iron fumarate, iron pyrophosphate, a porphyrin-iron complex, and an albumin incorporating porphyrin-iron complex.
US20120129914 Organic compositions to treat hsf1-related diseases The present disclosure relates to methods of treating heat shock factor 1 (HSF1)-related diseases such as cancer and viral diseases, using a therapeutically effective amount of a RNAi agent to HSF.
US20110091555 Use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant in the manufacture of a medicament for treating female genital disorders. A hydrophilic matrix is disclosed which comprises: a) at least one polyacrylic acid derivative in preferred amounts of 0.5-40%, b) at least one cellulose ether in preferred amounts of 30-90% and c) at least one disintegrant in preferred amounts of 2-50%, with respect to the weight of the matrix. This matrix is used in combination with at least one pharmaceutically acceptable active principle for manufacturing solid bioadhesive controlled release formulations for the treatment of vaginal disorders, such as vulvovaginal candidiasis, bacterial vaginosis or trichomoniasis. According to a preferred embodiment, the matrix is used in amounts of about 5-60% and the active principle in amounts of about 2-70%, with respect to the weight of the formulation.
US7879315 such as inositol phosphoric acid esters (phytic acid), polyphenols (Perilla frutescen var. crispa polyphenols), perilla extract comprising rosmarinic acid, phosphoric acids, edetic acid salts, tartaric acid, malic acid, citric acid, and glycolic acid An agent for dissolving dental calculus and/or dental caries, which comprises one or more kinds of substances selected from the group consisting of inositol phosphoric acid esters (e.g., phytic acid), polyphenols (e.g., Perilla frutescen var. crispa polyphenols), phosphoric acids, edetic acid salts, tartaric acid, malic acid, citric acid, and glycolic acid as an active ingredient. Dental calculus and/or dental caries can be conveniently dissolved in a short period of time.
CN101036649A Function of ascomycin used as the immunosuppressor The invention relates to immunology art to disclose the use of ascosin as immunosuppressor, in particular, the use for preparing drugs for treating autoimmune diabetes and skin allograft rejection. According to the invention, production cost for the ascosin is extremely low with excellent immunosuppression effect, thus the ascosin is a immunosuppression drug with high efficiency and low mammalian toxicity.
CN101584729A Pharmaceutical composition used for reducing blood fat A pharmaceutical composition used for reducing blood fat comprises the following components: honeysuckle flower, vitamin B complex, vitamin E, and minor elements of zinc, selenium, chromium, copper, molybdenum, iodine and manganese. The pharmaceutical composition is mainly suitable for the people suffering from high blood fat. The pharmaceutical composition is quite effective in reducing blood fat, and can be used for a long time or applied according to the treatment course.
WO2009097874A1 Amino acid formulations comprising cysteine, methionine and/or serine for the prevention of paracetamol-induced liver damage Disclosed are compositions comprising a combination of amino acids selected from: a) L-Cysteine with L-Methionine; b) L-Cysteine with L-Serine; c) L-Cysteine with L-Methionine and L-Serine; d) L-Methionine with L-Serine; or precursors or transporters of said amino acids, for the prevention of paracetamol-induced liver damage.
CN102784117A Gentamicin sulfate composition freeze-dried orally disintegrating tablet and preparation method thereof The invention provides a gentamicin sulfate composition freeze-dried orally disintegrating tablet and a preparation method thereof, relates to the technical field of medicines and medicine preparation methods, and mainly solves the problem that a gentamicin sulfate preparation in the prior art is poor in curative effect and inapplicable to children and patients having difficulty in swallowing. The gentamicin sulfate composition freeze-dried orally disintegrating tablet is prepared from components including, by weight, 20%-30% of gentamicin sulfate, 30%-60% of mannitol, 1%-3% of gelatin, 0.1%-0.15% of sucralose and 45%-60% of water for injection. The gentamicin sulfate composition freeze-dried orally disintegrating tablet prepared from the components according to the weight percent is simple in preparation process and composition, is applicable to the children and the patients having difficulty in swallowing, and has the advantages of rapidness in disintegration and effectiveness, sufficiency in medicine absorption, convenience in taking, fine taste and avoidance of the first-pass effect of livers.
US20090304683 Soluble Fragments of The Sars-Cov Spike Glycoprotein The invention relates to the spike protein from the virus (SARS-CoV) that is etiologically linked to severe acute respiratory syndrome (SARS); polypeptides and peptide fragments of the spike protein; nucleic acid segments and constructs that encode the spike protein, polypeptides and peptide fragments of the spike protein, and coupled proteins that include the spike protein or a portion thereof; peptidomimetics; vaccines; methods for vaccination and treatment of severe acute respiratory syndrome; antibodies; aptamers; and kits containing immunological compositions, or antibodies (or aptamers) that bind to the spike protein.
US20100136118 Calcium absorption enhancer The present invention provides a calcium absorption enhancer that places no burden on the body of a human or a domestic animal to which a calcium compound is administered and can increase the efficiency with which a calcium content is absorbed into the body by supplying calcium ions in the stomach or the like of the human or the domestic animal in a sustained-release manner after administration of the calcium compound. The calcium absorption enhancer of the present invention contains, as an active ingredient, water-soluble calcium particles that can release calcium ions in an aqueous solution in a sustained-release manner.
WO2006066323A9 Formulations and treatments for trichology a formulation for trichological treatment of a patient including, in a dosage in the range of 3 g to 8 g: phytosterols in the range of 200 mg to 2500 mg; the quantitative equivalent of Polygonum multiflorum root 4:1 in 70% EW in the range of 600 mg to 2600 mg; methylsulfonylmethane in the range of 500 mg to 2000 mg; and bovine colostrum in the range of 500 m to 2000 m .
EP1839651A1 Method for producing a water-insoluble amorphous or partially amorphous controlled release matrix In the preparation of a medicament dosage form (or its precursor) by extrusion, the dosage form comprises a matrix having properties determined by the extrusion process. The matrix contains (a) at least one active agent, (b) one or more polysaccharides (and their derivatives and complexes) and, optionally, (c) one or more saccharides (and their derivatives) and (d) other materials. An independent claim is included for the dosage forms as described above.
WO2011156900A3 Compounds, compositions and methods for treatment of multiple sclerosis The invention relates to compounds, compositions dosage forms and methods comprising 6-phenyl-4-pyridin-4-yl-3-(4-pyrimidin-2-yl-piperazin-1-yl)-pyridazine hydrochloride or a pharmaceutically acceptable salt thereof, and methods for treating multiple sclerosis in a subject using same.
EP1171121B1 Pharmaceutical compositions comprising dipeptidylpeptidase iv inhibitors for the promotion of growth Inhibitors of dipeptidyl peptidase IV and pharmaceutical compositions comprising these inhibitors are useful in the treatment of short stature due to Growth Hormone deficiency and for promoting GH-dependent tissue growth or regrowth.
US20120220637 Ophthalmologic Compositions And Use Mode Thereof The invention concerns a pharmaceutical composition characterized in that it contains a combination of a parasympatholytic agent, a sympathomimetic agent and a local anaesthetic. Such a composition may be injected into the anterior chamber of the eye before a cataract operation or instilled on the eye before laser treatment.
DE102007049157A1 New substituted 2,3-dihydro-(1,2,3)triazol-4-one compounds are hypoxia inducible factor-prolyl-4-hydroxylase inhibitor, useful for preparing medicament to treat and/or prevent e.g. cardiovascular diseases, inflammatory disease and anemia Substituted 2,3-dihydro-[1,2,3]triazol-4-one compounds (I), and their salts, solvates or solvates of the salts, are new. Substituted 2,3-dihydro-[1,2,3]triazol-4-one compounds of formula (I), and their salts, solvates or solvates of the salts, are new. R 1>a heteroaryl-group of formula (a), (b), (c), (d), (e) or (f); A : C-R 3>or N, where maximum two ring members of A represents N; D 1>O, S or N-R 4>; E : C-R 5>or N, where maximum two ring members of E represents N; R 2>a heteroaryl group of formula (i), (ii), (iii), (iv), (v), (vi), (vii), (viii), (ix), (x), (xi), (xii) or (xiii); G : C-R 7>or N, where maximum two ring members of G represents N; J : O, S or N-R 7>; L : C-R 8>or N, where maximum two ring members of L represents N; R 3>, R 6>, R 8>H or a substituent of the series of halo, CN, NO 2, (1-6C)-alkyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5-6-membered heteroaryl or L 1>; R 4>, R 7>H or a substituent of series of (1-6C)-alkyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5-6-membered heteroaryl (where in R 3>, R 4>, R 6>-R 8>: (1-6C)-alkyl is 1-3 times substituted by series of halo, CN, oxo, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5-6-membered heteroaryl, or L 1>, where cycloalkyl-, heterocycloalkyl-, phenyl- or heteroaryl-remainders are 1-3 times substituted by L 2>, and (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5-6-membered heteroaryl are 1-3 times substituted by a series of (1-6C)-alkyl, halo, CN, oxo or L 1>, where the alkyl group is 1-3 times substituted by L 3>); R 9>, R 1> 0>H, (1-6C)-alkyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5-6-membered heteroaryl, where (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5-6-membered heteroaryl are 1-3 times substituted by L 2>, and (1-6C)-alkyl is 1-3 times substituted by L 3>; either R 1> 1>, R 1> 3>, R 1> 4>, R 1> 6>, R 1> 9>, R 2> 1>, R 2> 4>-R 2> 6>, R 2> 8>-R 3> 0>R 9>; and R 1> 2>, R 1> 5>, R 1> 6>, R 1> 8>, R 2> 0>, R 2> 2>, R 2> 3>, R 2> 7>, R 3> 1>H or (1-6C)-alkyl, where (1-6C)-alkyl is 1-3 times substituted by halo, CN, OH, CF 3, (1-4C)-alkoxy, NH 2, mono-(1-4C)-alkylamino, di-(1-4C)-alkyl amino, hydroxycarbonyl and/or (1-4C)-alkoxycarbonyl; or R 1> 1>R 1> 2>, R 1> 4>R 1> 5>, R 1> 6>R 1> 7>, R 1> 8>R 1> 9>, R 2> 0>R 2> 1>, R 2> 1>R 2> 2>, R 2> 3>R 2> 4>, R 2> 6>R 2> 7>, R 3> 0>R 3> 1>5-6-membered heterocycloalkyl ring (1-3 times substituted by L 2>); L 1>-C(=O)-R 9>, -C(=O)-OR 1> 0>, -C(=O)-NR 1> 1>R 1> 1>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5>, -NR 1> 7>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O)-NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9>OR -NR 3> 0>R 3> 1>; L 2>halo, CN, (1-4C)-alkyl, CF 3, OH, (1-4C)-alkoxy, CF 3O, oxo, NH 2, mono-(1-4C)-alkyl amino, di-(1-4C)-alkyl amino, hydroxycarbonyl and/or (1-4C)-alkoxycarbonyl; L 3>halo, CN, OH, CF 3O, (1-4C)-alkoxy, NH 2, mono-(1-4C)-alkyl amino, di-(1-4C)-alkyl amino, hydroxycarbonyl, (1-4C)-alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl and/or 5-6-membered heteroaryl; and R 5>H or a substituents of series of halo, CN, NO 2, (1-6C)-alkyl, CF 3, OH, (1-6C)-alkoxy, CF 3O, NH 2, mono-(1-6C)-alkylamino, di-(1-6C)-alkyl amino, hydroxycarbonyl or (1-6C)-alkoxycarbonyl. Independent claims are included for: (1) the preparation of (I); and (2) a medicament comprising (I), in combination with an inert, non-toxic, auxiliary material and one or more further active substances of angiotensin-converting enzyme-inhibitor, angiotensin II-receptor antagonist, beta-receptor-blocker, calcium-antagonist, phosphodiesterase-inhibitor, mineralocorticoid-receptor-antagonist, diuretics, aspirin, iron-supplements, vitamin B12- and folic acid-supplements, statin, digitalis (digoxin)-derivative, tumor-chemotherapeutics or antibiotics. [Image] [Image] [Image] [Image] [Image] - ACTIVITY : Cardiovascular-Gen.; Cardiant; Antianemic; Nephrotropic; Vulnerary; Antimicrobial; Anti-HIV; Antiinflammatory; Antiarthritic; Anti
CN102793664A Sodium aescinate micro-emulsification injection and preparation method thereof The invention discloses a sodium aescinate micro-emulsion injection. The formula of the sodium aescinate micro-emulsion injection comprises sodium aescinate, an oil phase, a surfactant and a cosurfactant. Compared with the oral gavage, the sodium aescinate micro-emulsion injection for intravenous injection provided by the invention has the advantages that the bioavailability is high, the concentration of the injection in the liver can be increased obviously, the concentration of the injection in the kidney can be reduced, meanwhile, the irritation on the wall of the blood vessel is alleviated, and the generation times of phlebophlogosis can be reduced, so that the curative effect is improved, and the toxic and side effect is lowered.
WO2013169727A1 Polymorphic salt of the oxalate salt of 6 - o - ( 4 - dimethylaminoethoxy) cinnarnoyl fumagillol and methods of making and using same The disclosure is in part directed to crystalline forms of an oxalate salt of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol.
CN101347411A Ibuprofen suspension and method of preparing the same An ibuprofen suspension and a preparation method thereof relate to medicines, in particular to the pharmaceutical technical field of chemical drugs. The preparation method comprises the following steps: sucrose and an antiseptic are mixed with purified water to produce simple syrup, the ibuprofen is moistened in a moistening agent; suspending agents are respectively swelled; then the three mixtures are mixed and ground with glycerol, a deflocculating agent and the purified water to produce grinding liquid; the grinding liquid, the simple syrup, the antiseptic and a corrective agent are added into a liquid preparation tank and stirred evenly, thus the ibuprofen suspension is obtained. The ibuprofen suspension and the preparation method thereof have the advantages of simple process, being easy for manufacturing and operation, high qualification rate of the finished product, good drug effect and being easy for storage; the ibuprofen suspension has no spicy taste, is convenient to be taken by children, and can be directly absorbed by human body without disintegration and dissolution, thus the drug can be absorbed quickly and has quick effect.
US20100298403 MODIFIED POLY(PROPYLENE-IMINE) DENDRIMERS AND THEIR USE AS TRANSFECTION AGENTS FOR AMIONIC BIOACTIVE FACTORS ( as amended The present invention is concerned with modified poly-(propylene imine) dendrimers, comprising cationic internal ammonium groups and external non-toxic endgroups, pharmaceutical compositions comprising said dendrimers, methods for the production of said dendrimers and their use as transfections agents for anionic bioactive therapeutic factors, for use in gene therapy, in particular for the treatment of cancer. The modified poly-(propylene imine) dendrimer of generation 1, 2, 3, 4 or 5, also comprising incomplete dendrimers and mixtures thereof, comprising external end groups and internal amine functions are characterized in that: (a) substantially all external endgroups are groups of formula (I) wherein R is a radical selected from the group of C1-10alkyl, polyethylene glycol radical and polyethylene glycol gallyl radical; and (b) substantially all internal amine functions are quaternary cationic ammonium functions. Most preferred are the quaternized compounds DAB-dendr-(NHCOCH3)4, DAB-dendr-(NHCOCH3)8, DAB-dendr-(NHCOCH3)16, DAB-dendr-(NHCOCH3)32, DAB-dendr-(NHCOCH3)64, DAB-dendr-(NHCOPh((EO)4OMe)3)4, DAB-dendr-(NHCOPh((EO)4OMe)3)8, DAB-dendr-(NHCOPh((EO)4OMe)3)16, DAB-dendr-(NHCOPh((EO)4OMe)3)32 and DAB-dendr-(NHCOPh((EO)4OMe)3)64.
WO2006105665A1 Hydrogel composition for modulation of topical inflammatory response A hydrogel composition comprising a biocompatible polymer component, a protein component and one or more cytokines is provided. The invention also relates to a cosmetic method of preventing or reducing scarring that includes applying a hydrogel composition to an open wound. Novel uses of a hydrogel composition in the manufacture of a medicament for the treatment of topical inflammation also are disclosed.
EP2521544A2 Topical transdermal dexmedetomidine compositions and methods of use thereof Analgesic topical formulations of dexmedetomidine and methods of use thereof in the treatment and management of pain and other conditions.
US20100249189 Nitric oxide donor compounds The invention relates to nitric oxide donors of the formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: wherein A and A′ are independently selected from the group consisting of H and —(X)S—Y with the proviso that at least one of A or A′ is not H; wherein s is 0 or 1; X is selected from the group consisting of: —CO—, —COO—, —CONH— and —SO2— or Y is straight or branched C1-C20 alkyl chain, preferably C1-C10 alkyl chain, substituted with one or two —ONO2; or C1-C6 alkylenoxy-C1-C5 alkyl wherein the alkyl group is substituted by one or two —ONO2 groups. The invention also provides novel compositions comprising at least one compound of the invention and at least one therapeutic agent.
CN101993373A Chlorinated glaucocalyxin A derivative and preparation method and application thereof The invention discloses a structure and a preparation method of a chlorinated glaucocalyxin A derivative, and application of the chlorinated glaucocalyxin A derivative to the treatment of cancer thereof. The general molecular structural formula of the chlorinated glaucocalyxin A derivative is shown below, wherein R1 is benzoyl chloride substituent(-C7H6O2), benzene sulfonyl chloride substituent(-C6H6O3S2) or -OH; and R2 is benzoyl chloride substituent(-C7H6O2), benzene sulfonyl chloride substituent(-C6H6O3S2) or -OH. The preparation method is to prepare the disclosed chlorinated glaucocalyxin A derivative by reacting the extracted glaucocalyxin A with benzoyl chloride or the benzene sulfonyl chloride in the presence of triethylamine and 4-dimethylamino pyridine.
CN103271883A Preparation method for pazufloxacin mesilate for injection The invention provides a preparation method for pazufloxacin mesilate for injection. The preparation method comprises the following steps of: preparing the pazufloxacin mesilate and mannitol according to a prescription, and regulating pH values to be 3.0-4.0; adding a proper amount of needle active carbon, heating the mixture to be 70-80 DEG C, and carrying out decoloring after stirring for 15-20 minutes; putting an encapsulated semi-finished product into a freezing vacuum drier, controlling the temperature to be below -30 DEG C and carrying out prefreezing for 1-1.5 hours; when the temperature of a cold trap of the drier is lower than -40 DEG C, vacuumizing until the pressure is 20 Pa, and carrying out constant-temperature drying for 0.5-1 hour; raising the temperature of a separation board of the drier to be -10 DEG C, carrying out the constant-temperature drying for 0.5-1 hour; and raising the temperature of the separation board to be 0 DEG C, carrying out the constant-temperature drying until the waterline of the product reaches the bottom, raising the temperature to be 10 DEG C in a temperature manner, after carrying out the constant-temperature drying until the temperature of the product approximates to 0 DEG C, raising the temperature of the separation board to be 35 DEG C, and judging that the product is qualified after carrying out the constant-temperature drying until reaching the end point. The preparation method has the advantages that the production cost is lowered and the product quality is improved and is more suitable for industrial production.
US20090054433 Pharmaceutical compositions containing quinazoline derivatives for treating as serotonin receptor antagonist The present invention relates to a pharmaceutical composition containing one or more quinazoline compounds as an active ingredient, which has antagonistic activity against serotonin 5-HT3A and is effective for the prevention and treatment of central nervous system (CNS) diseases, including emesis, nausea, alcoholism, drug abuse, depression, compulsive neurosis, anxiety, seizure, Alzheimer's disease, Parkinson's disease, Huntington's chorea, psychosis, schizophrenia, suicidal tendency, sleep disorder, appetite disorder and migraine.
US20080300200 Therapeutic Furopyrimidines and Thienopyrimidines The invention provides compounds of formula I, II, and III as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of formula I, II, and III are useful as anti-viral agents and/or as anti-cancer agents.
WO2012142117A1 Solid state forms of cabazitaxel and processes for preparation thereof The invention relates to solid state forms of Cabazitaxel, and processes for preparation, via novel synthetic intermediates, thereof, and formulations comprising one or more of the solid state forms of Cabazitaxel. The present invention further provides pharmaceutical compositions comprising one or more of the solid state forms of Cabazitaxel, and a method of treating hormone-refractory prostate cancer.
EP2753312A1 Use of an aromatase inhibitor for the treatment of hypogonadism and related diseases This invention relates to a method of increasing testosterone levels and treating hypogonadism and related diseases with the aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile. The present invention further relates to a method of increasing testosterone levels and treating hypogonadism and related diseases with the aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile in a particular dosing regimen. The invention also relates to pharmaceutical compositions comprising said aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile, optionally in combination with other active ingredients. Furthermore, the present invention relates to kits comprising said pharmaceutical compositions together with instructions how to administer them.
WO2012021981A1 Novel phytochemicals from extracts of maple syrups and maple trees and uses thereof The present invention describes phytochemicals present in maple syrup and maple tree extracts by butanol, ethyl acetate and methanol. Novel compounds are isolated from maple syrups, including one compound Quebecol generated in the maple syrup manufacturing process. Also described are digesting extract of maple syrup. The phytochemicals may be used for the treatment or prevention of cancers, metabolic syndromes, diabetes, microorganism infections and/or antioxidants.
US20080050479 Food product & process for manufacturing same There is provided a commercially packaged mammal pet food product that includes a manufactured, shelf-life stable food substrate and a combination of functional additives. The functional additives include at least one non-palatable plant-based remedy and/or dietary fiber source that are present to strengthen and/or maintain a specified health indicator of a mammal pet animal. The food product is portioned and packaged with the functional additives being present in predetermined concentrations and amounts sufficient to be effective in achieving said indications on regular feeding of the pet animal with said food product. The food substrate is present in a proportion sufficient to mask the flavor and/or odor of the non-palatable additive and is made-up of a unique combination of materials that are able to be processed at lower temperatures to preserve the natural botanical functional additive's activity.
US20090274741 Polymers containing poly(ester amides) and agents for use with medical articles and methods of fabricating the same Polymers containing poly(ester amides) and agents for use with medical articles and methods of fabricating the same are disclosed. The medical article generally comprises an implantable substrate having a coating, and the coating contains a polymer comprising a polymeric product of a reaction comprising a polyol, a polycarboxylic acid, an amino acid and an agent.
US20120034319 Antimicrobial hydrochloric acid catheter lock solution and method of use A catheter lock solution includes a hydrochloric acid solution having a concentration of 0.3 Molar to 1.0 Molar. This hydrochloric acid solution may be used to lock a catheter and/or salvage an infected catheter.
CN1850836A Celosia argentea suponin compound and its pharmaceutical use This invention relates to natual medicine chemical and medical technique field. It discloses two kind celosin new compounds of celosin A and celosin B structure and its distillation and eperating method from amaranthcea plant celosin. Their chemical general formula is shown as formula (1). This invention also discloses the compound and its derivative medicine aspect application of curing and preventing fatty liver, liver injury, hepatic fibrosis, liver cirrhosis, coronary heart disease, cardiac infarction, myocardial ischemia, cerebral ischemia, cerebral infarction, cerebral apoplexy, diabetes mellitus, hyperinsulinism, insulin resistance disease, obesity, glucose intolerance capability, and/or hypertension adiposity, hyperlipemia, dementia, depression or anxiety, and insomnia diseases.
US20120076735 Nanoparticles for Extravascular Administration Disclosed are drug delivery systems and methods for extravascular administration of drug, vaccine, and/or diagnostic agents, for use in research and medical applications.
CN101497584A Isoquinoline-3-formyl amino acid formyl amino acid benzyl ester, as well as preparation and use thereof The invention discloses an isoquinoline-3-formyl amino acid benzyl ester with a general formula I of anti-tumor activity or a pharmaceutically acceptable salt thereof. As shown in the general formula I, AA is alanine(Ala), glycine(Gly), leucine(Leu), isoleucine(Ile), valine(Val), phenylalanine(Phe), serine(Ser), threonine(Thr), tyrosine(Tyr), benzyloxy-aspartic acid(Asp(OBzl)), benzyloxy-glutamic acid(Glu(OBzl)), asparamide(Asn), glutamine (Gln), methionine(Met), proline(Pro), tryptophan(Trp), histidine(His) or lysine(Lys).
EP2042178A1 Ocular formulations comprising 5-chlorouracil and use thereof The present invention is related to new ocular formulations. In particular, the invention provides a use of 5-chlorouracil for the preparation of a pharmaceutical composition for the treatment of glaucoma, especially associated with glaucoma filtering surgery. More particularly, the present invention provides novel pharmaceutical compositions of 5-chlorouracil and use of these in the preparation of pharmaceutical compositions for the treatment of glaucoma, especially associated with glaucoma filtering surgery.
US7195914 Composition and method for treatment of hypertriglyceridemia A polyunsaturated fatty acid-containing composition for treating hypertriglyceridemia and methods of use thereof are provided.
WO2011056486A2 Devices, methods, and composition for controlling infections The subject invention provides novel and highly effective methods and devices for convenient and effective wound irrigation.
US20110059951 HETEROCYCLIC DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS The present invention provides heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
CN1615857A Amlexanox double layer oral patches and its preparing method The double layer Amlexanox oral patch includes two layers, one adhered Amlexanox layer with Amlexanox in 0.1-10 mg and the other water insoluble protecting layer. The double-layer design reduces the dissolving of medicine to the side opposite to the oral cavity mucous membrane and reduces the bi-directional adhesion between gum and oral cavity mucous membrane, makes most of the medicine penetrate to the ulcer surface and decreases the upset in the oral cavity. The double layer Amlexanox oral patch is located to the ulcer focus, has no irritation to the ulcer surface and acting period as long as 3-4 hr.
CN101239057A Use of salvianolic acid B and its salt in treating parkinson's disease The invention relates to a new usage of Salvianolic acid B and the salt used in curing parkinsonism, the usages of the medicine combined material of the Salvianolic acid B as well as the salt, and the medicine combined material or each unit being jointly used with other current medicines curing parkinsonism used for curing parkinsonism.
US20100173937 Use of tetrakis-quaternary ammonium salts as pain modulating agents Provided are methods of modulating, treating, reversing and/or preventing pain using tetrakis quaternary ammonium compounds, especially regarding pain of central and/or peripheral origin and/or pain which is nociceptive, neuropathic, somatic, visceral, and/or inflammatory in nature.
CN101953803B Preparation method of small-volume doxofylline freeze-dried powder injection and device thereof The invention discloses a preparation method of a small volume doxofylline freeze-dried powder injection. The preparation method is characterized by comprising the following steps: weighing doxofylline and auxiliary materials of the prescription amount, and adding the injection water of 80 to 90 DEG C to prepare a concentrated solution, and fully stirring so as to dissolve the materials; adding active carbon, stirring uniformly the mixture, heating to boil, and filtering; adding the dilute solution which is prepared by the residual injection water of 80 to 90 DEG C into the filtrate, keeping the temperature no lower than 80 DEG C, fully stirring, carrying out micro-filtering, and continuing to keep the temperature not lower than 80 DEG C; and filling into a 20ml ampoule, freeze-drying, pressing and sealing to obtain the product. The method of the invention has the beneficial effect of effectively reducing the packaging size so as to lower the packaging cost and the transport cost, andgreatly reducing the energy consumption of the freeze-drying and evaporating so as to reduce the cost further due to that the preparation amount filled into the ampoule is only 7 to 8 ml before the freeze-drying.
EP1539128B1 Use of skin-protecting substances The invention relates to the use of at least one substance which can form a zwitterion and/or the derivatives thereof for protecting the skin.
CN1923232B Medicine composition for dispersing pathogenic wind and extinguishing phlegm, absorbing clots and softening hard masses, preparation method and use thereof The invention discloses a pharmaceutical composition for dispersing pathogenic wind, removing phlegm, its preparing process and use thereof, wherein the composition is prepared from centipede, pangolin scales, white-stiff silkworm, buthus martensi karsch, turtle shell, tortoise shell, orpiment, rhubarb horsetails and cinnabar. The The medicinal composition can be prepared into capsules, powders, tablets, granules, pills, mixtures and oral liquids.
WO2009117987A2 Use of boswellia acids and synthetic boswellia acid derivatives for inhibiting microsomal prostanglandin e2 synthase and cathepsin g The present invention relates to new boswellia acid derivatives. The present invention furthermore relates to the use of preparations with boswellia acid derivatives or synthetic derivatives, especially with boswellia acid derivatives, which are esterified or etherified at the C3-OH function, for inhibiting the induceable microsomal prostaglandin E2 synthase-1 and/or for inhibiting cathepsin G. Furthermore, the invention relates to the use of boswellia acids or synthetic derivatives for the preparation of a drug for the treatment of PGE2- and/or cathepsin G-induced pathological conditions.
US20100041736 Isolated MCPIP and Methods of Use A monocyte chemoattractant protein (MCP-1)-inducible protein, MCPIP, its polynucleotide and amino acid sequences from mouse and human, and methods for its use are disclosed.
CN101293102A Non-virogene carrier for complexation platinum series antineoplastic medicament and preparing method thereof The invention relates to a non-viral gene drug carrier of a complexing platinum-based anti-tumor drug, which is the Pt-PEI-PEG or PEG-PEI-Pt complex carrier, PEI is taken as a framework to connect polyethylene glycol and complex the platinum anti-tumor drug for constitution; and the molar percentage of all the components of the complex are: Pt: 48.8 to 83.2 percent, PEI: 16.5 to 49.8 percent, PEG: 0.17 to 2.44 percent respectively. The preparation method is that the platinum compound and the PEI are carried out the coordination, the reaction with the PEG is further carried out, thus generating the Pt-PEI-PEG complex carrier; or the platinum compound and the PEG-PEI complex are carried out the coordination reaction, thus generating the PEG-PEI-Pt complex carrier. The non-viral gene drug carrier has the advantages of effects of the anti-tumor drug, high stability, good water solubility, long cycle in vivo and lowering toxicity.
US20080199414 Tiliroside or derivative; drugs, foods; ultraviolet radiation filters; aging and oxidation resistance; free radical scavengers; antiinflammatory, anticarcinogenic, and antiallergen agents; plant extracts; topically applied The invention relates to cosmetic formulations, pharmaceutical preparations, food products and food supplements containing flavonoid derivatives. The flavonoid derivatives act therein, for instance, as UV filter. Some flavonoid derivatives represent novel compounds.
WO2014034719A1 Quinoline derivative having tlr inhibitory activity A compound represented by general formula (1), a salt of the compound, or a solvate of the compound or the salt, which can inhibit TLR3, 7 and/or 9 and has an excellent prophylactic and/or therapeutic effect on autoimmune diseases, inflammations, allergies, asthma, graft rejection, GvHD or cardiomyopathy associated with sepsis. A: a (substituted) 5- to 6-membered saturated nitrogen-containing heterocyclic ring; Y: a bond or a phenylene group; Z: a bond, a C1-6 alkylene group, N-R7 or O; R1, R3 and R5 to R8: H, a C1-3 alkyl group or the like; R7: H, a C1-6 alkyl group or a 2-nitrobenzenesulfonyl group; and R2 and R4: one represents R8 and the other represents a group represented by formula (2) (wherein B: a (substituted) carbocyclic/heterocyclic ring, W: a C2-6 alkenylene group or the like, X, V: a bond, C(O)NH, NHC(O) or the like, and U: a bond or a C1-6 alkylene group; wherein a case in which each of X, V and U is a bond is excluded).
US7145015 Benzocycloheptenes, process for their production, pharmaceutical preparations that contain that latter as well as their use for the production of pharmaceutical agents Benzocycloheptenes of formula (I), in which R1, R2 and Y have the meanings that indicated herein, exhibit selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis:
CA2566937A1 Substituted 2,5-diaminomethyl-1h-pyrroles The invention relates to substituted 2,5-diaminomethyl-1 H-pyrroles, to a method for the production thereof, to medicaments containing said compounds and to the utilization of these compounds for the production of medicaments.
US6984646 suitable for the preparation of medicaments for the treatment of diseases associated with p38 MAP kinase such as atherosclerosis, diabetes, adult respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease (COPD), asthma, fever etc The invention relates to imidazopyridinones of the formula wherein the groups R1, R2, R3, and R4 are as defined in claim 1, to the process for their preparation, to pharmaceutical compositions containing them, and to a method of using them for treatment of chronic inflammatory processes in humans or animals.
US20050142173 Testosterone hydroalcoholic gel for transdermal use; unique pharmacokinetic steady-state profile for testosterone A pharmaceutical composition useful for treating hypogonadism is disclosed. The composition comprises an androgenic or anabolic steroid, a C1-C4 alcohol, a penetration enhancer such as isopropyl myristate, and water. Also disclosed is a method for treating hypogonadism utilizing the composition.
US6969760 Jak kinases and regulation of cytokine signal transduction The invention relates generally to the Jak family of kinases. This includes the DNA and amino acid sequences for Jak 3 kinases. Additionally, the invention concerns expression vectors comprising DNA sequences encoding a Jak 3 kinase and host cell containing such expression vectors.
WO2009078746A1 Substituted 3 -hydroxypyridines and pharmaceutical compositions thereof The present invention relates to novel therapeutic compounds of formula (I) wherein R1 is selected from the group consisting of C2-8alkyl, R2 is independently selected from the group consisting of C1-8alkyl, R3 is independently selected from the group consisting of H and C1-8alkyl, R4 is independently selected from the group consisting of C1-8alkyl or pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the same, the compounds for use as medicaments, and use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. The novel compounds are useful for the treatment of age-related disorders accompanied with dysfunctional insulin receptor signaling.
CN103536592A Metronidazole-furazolidone vaginal expandable suppository and its preparation method and detection method The invention relates to a metronidazole-furazolidone vaginal expandable suppository and its preparation method and detection method. The metronidazole-furazolidone vaginal expandable suppository comprises a drug-containing matrix comprising active components and a matrix, and also comprises an expandable carrier. The active components comprise metronidazole and furazolidone. The active components further comprise alum, borneol and frankincense. A clathrate is prepared from metronidazole and hydroxypropyl-beta-cyclodextrin. A solid dispersion is prepared from furazolidone, alum, frankincense, borneol and a sustained-release material. The metronidazole-furazolidone vaginal expandable suppository comprises a quick release part and a slow release part and has effects of fast and stably inhibiting bacteria. The metronidazole-furazolidone vaginal expandable suppository is a hollow two-layer expandable suppository and thus suppository stability is improved. The metronidazole-furazolidone vaginal expandable suppository adopts seven unique technologies and has the advantages of drug liquid flowing-out prevention, high stability, long action time and secondary infection prevention.
EP1792625A1 Use of a phosphatidylserine/polypeptide conjugate for inducing autoimmunity in the treatment of cancers Disclosed are methods and compositions for the prevention and treatment of cancers using lipid-carrier protein conjugate compositions for generating lipid-specific immune responses in an animal. Also disclosed are methods for making phosphatidylserine conjugate compositions and their formulation for use in a variety of pharmaceutical applications including the detection and treatment of a variety of cancers and related conditions.
CN101766575A Dropping pill with fentanyl as main active component and preparation method thereof The invention relates to a dropping pill with fentanyl as a main active component and a preparation method thereof. The dropping pill adopts the fentanyl and salts or hydrates which can be accepted in terms of pharmacy as the active components. The invention aims at providing a new preparation namely the fentanyl dropping pill for vast patients and medical workers. The fentanyl dropping pill has the following characteristics: the disintegration is quick, the bioavailability of the pill can be enhanced, the curative effect of the pill can be completely exerted, and adverse reactions can be reduced; the fentanyl dropping pill is convenient not only for children to take, but also for old people to take with reduced dosage; the preparation method is simple; in addition, the fentanyl dropping pill is suitable for mass production and is convenient for carrying, storing as well as transporting. The fentanyl and the salts or the hydrates which can be accepted in terms of pharmacy are adopted as the active components and some accessories of specified categories and in specified proportions are added, so as to prepare the dropping pill according to the conventional technology in terms of pharmaceutics.
WO2014138556A1 Kits and methods for the treatment of cancer using gliadin peptides Kits and methods for treating cancer comprising administration of a gliadin peptide to a patient are disclosed herein. A kit according to the invention comprises a pharmaceutical composition comprising a gliadin peptide and instructions for administering the peptide to a patient. The kit may further comprise a pharmaceutical composition comprising at least one chemotherapeutic agent such as a receptor tyrosine kinase inhibitor and instructions for co¬ administering the compounds. A method of treating cancer according to the invention comprises administering a gliadin peptide to a patient and may further comprise co-administering at least one chemotherapeutic agent such as a receptor tyrosine kinase inhibitor. Co-administration of a gliadin peptide and receptor tyrosine kinase inhibitor to a patient with cancer is effective to decrease or prevent resistance of the cancer to the receptor tyrosine kinase inhibitor.
CN101972384B Plaster for treating acute soft tissue injury and preparation method thereof The invention discloses plaster for treating acute soft tissue injury. The medicinal active ingredients of the plaster comprise the following raw materials in part by weight: 55 to 65 parts of fried gardenia jasminoides, 55 to 65 parts of rhubarb, 55 to 65 parts of airpotato yam rhizome, 25 to 35 parts of frank incense, 25 to 35 parts of myrrh, 25 to 35 parts of common monkshood mother root, 25 to 35 parts of kusnezoff monkshood root, 25 to 35 parts of safflower and 5 to 15 parts of borneol. The invention also discloses a preparation method of the plaster. The plaster can relieve the acute pain and swelling of the acute soft tissue injury quickly, contributes to recovery of functions, takes effect quickly, is convenient to use and has the effects of clearing heat and releasing toxin, promoting blood circulation and dispersing blood stasis and eliminating swelling and stopping pain.
CN103142604A Acetaminophen and caffeine dispersible tablet, and its preparation method The invention discloses an acetaminophen and caffeine dispersible tablet, and its preparation method. The acetaminophen and caffeine dispersible tablet comprises medicinal active components and preparation auxiliary materials; the medicinal active components are composed of acetaminophen and caffeine according to a acetaminophen/caffeine weight ratio of 1:0.13; and the preparation auxiliary materials comprise a filler, a disintegrant, a diluent, a lubricant, a flow aid and a flavoring agent. The disintegrant is composed of polyvinylpyrrolidone and sodium carboxymethyl starch according to a polyvinylpyrrolidone/sodium carboxymethyl starch weight ratio of 3-1:0.2-1. The acetaminophen and caffeine dispersible tablet has the advantages of rapid dissolve-out, fast absorption, high bioavailability, good stability, taking convenience and the like.
WO2011051899A1 A synergistic composition of (-)-hydroxycitric acid with monoterpene and a method to enhance satiety The present disclosure provides synergistic composition comprising (-)-hydroxycitric acid, its salts, amides and esters in conjunction with monoterpenes for enhancing satiety. The disclosure is also related to the use of synergistic composition in food and pharmaceutical compositions. The present disclosure helps in controlling obesity by enhancing satiety.
CN103110949A Ribavirin small-capacity injection preparation and preparation method thereof The invention discloses a ribavirin small-capacity injection preparation. The ribavirin small-capacity injection preparation comprises the following components in percentage by weight: 5%-15% of ribavirin, 1%-4% of anodyne, 0.01%-0.03% of active carbon, and water being supplemented to 100% by weight, wherein the pH value is regulated to 5.0-6.0 by a buffer solution. The invention further discloses a preparation method of the ribavirin small-capacity injection preparation. The ribavirin small-capacity injection preparation is detected and checked by regulating the dosage ratio of the anodyne, active carbon and the buffer solution in the prescription, and carrying out primary filtration, intermediate filtration and refined filtration by adopting a titanium rod filter, a 0.65-micron polypropylene filter core and a 0.22-micron polyether sulfone filter core in sequence, so that the defects of large primary medicine consumption and low percent of pass during the preparation process of the ribavirin small-capacity injection preparation are effectively solved. Besides, the prescription is simple, the yield is high, the clinical application is safe, the pain feeling is small, and the large-scale industrial production is convenient.
US20110264043 Method of loading a drug library into an infusion pump A method of loading a drug library into an infusion pump includes transferring the drug library, stored on a remote device, to the infusion pump via a wireless connection. The drug library includes a plurality of subdirectories, and each subdirectory includes a care area, at least one drug, data associated with and dependent upon the drug(s), and at least one mode of operation for infusing the drug(s).
US7534897 Indole arylsulfonaimide compounds exhibiting PGD 2 receptor antagonism A compound having CRTH2 receptor antagonism, represented by the following formula (I). The compound is useful for the treatment of allergic diseases having a relation to eosinophils and the like. A compound of the formula (I): wherein a group represented by the formula: is a group represented by the formula: and the like, R1 is carboxy and the like, R3 is —(CH2)n-N(—Y)—SO2—Ar and the like, the other symbols are as defined in claim 1.
CN102895188A Borneol-curcumin liposome and preparation method and application thereof The invention belongs to the medicine field and provides a borneol-curcumin liposome, a preparation method of the borneol-curcumin liposome and an application of the borneol-curcumin liposome in preparing medicines for preventing human immunodeficiency virus-1(HIV-1) associated neurocognitive disorder. The borneol-curcumin liposome is prepared by, by mass, 270-330 parts of lecithin, 90-110 parts of cholesterol, 0.9-1.1 parts of curcumin and 0.09-0.11 part of borneol. The preparation method includes that the components and 0-11 parts by mass of oxidation protection agents are dissolved by absolute ethyl alcohol, a mixture is subjected to rotary evaporating on a rotary evaporator until ethanol is volatilized to form uniform films, a defined amount of phosphate buffer solution is added, the incubation is performed for three hours, a hydration reaction is undertaken to form an emulsion, then the ultrasound is performed for 10 minutes, and the emulsion passes through a 0.45 micrometer millipore filter to obtain uniform particles so that the borneol-curcumin liposome is obtained. The borneol-curcumin liposome can be prepared to various dosage forms of HIV-associated neurocognitive disorder (HAND) resistant medicines which are peroral, and the pertinence of the borneol-curcumin liposome for treating HAND is high, and the effect is good.
WO2007013290A1 Anti-inflammatory analgesic agent Disclosed is an anti-inflammatory analgesic agent which is excellent in safety and has excellent anti-inflammatory effect and/or analgesic effect. An anti-inflammatory analgesic agent comprising a carpronium salt (3-(methoxycarbonylpropyl)trimethyl ammonium salt); a method for treatment/prevention of an inflammation and/or a pain using the analgesic agent; and use of a carpronium salt for the preparation of the anti-inflammatory analgesic agent.
EP1183243B1 Short-acting benzodiazepines It has now been found that compounds of the present invention as described in Benzodiazepine derivatives of Formula (I) containing a carboxylic ester moiety and thereby capable of being inactivated by nonspecific tissue esterases in an organ-independent elimination mechanism and thereby providing a more predictable and reproducible pharmacodynamic profile. The compounds of the present invention are suitable for therapeutic purposes, including sedative-hypnotic, anxiolytic, muscle relaxant and anticonvulsant purposes and are useful to be administered intravenously in the following clinical settings: preoperative sedation, anxiolysis, and amnestic use for perioperative events; conscious sedation during short diagnostic, operative or endoscopic procedures; as a component for the induction and maintenance of general anesthesia, prior and/or concomitant to the administration of other anesthetic agents; ICU sedation.
CN103356661A Novel capsule filled with metformin hydrochloride solid preparation and glipizide solid preparation The invention relates to an oral-taking hard capsule, and in particular relates to a tablet capsule filled with a metformin tablet and a glipizide tablet. The tablet capsule comprises a capsule and tablets in the capsule, wherein the capsule contains an upper capsule body and a lower capsule body; at least one tablet taking metformin as an active component and at least one tablet taking glipizide as an active component are filled in the capsule. According to the tablet capsule filled with the metformin tablet and the glipizide tablet, various active components in the capsule are not in contact with each other, thus the tablet capsule with good stability and convenience for processing is obtained.
US7534913 Crystalline form of nateglinide Provided are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, α, β, γ, δ, ε, σ, θ and Ω, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.
EP2535332A1 Sinomenine derivatives, synthetic methods and uses thereof The invention relates to sinomenine derivatives, methods for their synthesis and their applications. The sinomenine derivatives include oxidation derivatives, and C-10 substituted sinomenine derivatives. Based on the readily oxidizable phenol group on sinomenine structure, using oxidation, oxidative dearomatization, or conjugated addition aromatization, one can introduce C-10 substitutions to synthesize the sinomenine derivatives. The sinomenine derivatives of the invention have the following structures: Using in vitro TNF-α inhibition assay, the activities of the synthetic compounds are assessed. Results from these assays shown that most compounds have anti-inflammatory effects, and some compounds have better activities than that of sinomenine. These compounds may be used in treating immune diseases such as rheumatoid arthritis (RA).
CN103214542A B-nor-6-(4'-alkyl) aminothizone cholestane compound, and preparation method and application thereof in anticancer drugs The invention discloses a B-nor-6-(4'-alkyl) aminothizone cholestane compound, which has a chemical formula shown in the specification. The B-nor-6-(4'-alkyl) aminothizone cholestane compound disclosed by the invention is prepared from cholesterol by using the chemical methods such as functional group protection, ozonation, cyclization, condensation, deprotection, oxidation and addition. Experiments prove that the B-nor-6-(4'-alkyl) aminothizone cholestane compound disclosed by the invention has an obvious inhibitory effect on various tumor cells, and can be applied to the preparation of drugs for treating cancers.
WO2006090932A1 Surrogate marker for sulfonamide compound A method of evaluating the effect of a sulfonamide compound on the expression of integrin which involves: (a) the step of measuring the expression amount of integrin in platelets collected from a patient to whom the above-described sulfonamide compound has been administered; and (b) the step of evaluating the effect of the above-described compound on the expression of integrin in cells other than the platelets based on the expression amount measured above.
CA2733790A1 Macrocyclic compounds for inhibition of tumor necrosis factor alpha The invention provides macrocyclic compounds of formula (I) and methods for their synthesis and use. In particular, the invention provides macrocyclic compounds that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.
US20100048720 Process for the Preparation of and Crystalline Forms of Optical Enantiomers of Modafinil The invention relates to a polymorphic form of (−)-modafinil that produces a powder X-ray diffraction spectrum comprising intensity peaks corresponding to interplanar spacings of about 14.14, 10.66, 7.80 and 4.02 Å, and a process for the preparation thereof.
CN102784163A Edible fungi compound polysaccharides health care treatment formula and preparation method thereof The invention relates to an edible fungi compound polysaccharides health care treatment formula and a preparation method thereof. The formula comprises the following raw materials according to part by weight: 20 to 60 parts of agaricus blazei murill polysaccharide, 10 to 30 parts of shii-take polysaccharide, and 5 to 15 parts of Indian buead polysaccharide. The edible fungi compound polysaccharides health care treatment formula is helpful to enhancing the immune function of a human body, improving the hematogenesis function of human bone marrow, and resisting cancers, has the effects of tonifying the liver and the kidney, strengthening the spleen and the stomach, maintaining beauty to keep young, clearing damp and promoting diuresis, and plays the role of relieving symptoms and treating for people suffering from the diseases such as cancers, anaemia, low resistance, hyperlipemia, hypertension, arteriosclerosis, diabetes, nephritis, difficult urination, oedema, edema, abdominal pain and diarrhoea.
EP1368004B1 Mucoadhesive dispersible pharmaceutical preparation for active-agent dosing in veterinary and human medicine The invention relates to a mucoadhesive dispersible pharmaceutical preparation for active-agent dosing in veterinary or human medicine comprising at least one active agent, characterised in that the preparation comprises a mucoadhesive matrix, which may be dispersed in aqueous media, containing at least one matrix-forming polymer, in which at least one active agent is dissolved or dispersed. The preparation disperses or is broken down within a maximum of 15 minutes after introduction into an aqueous medium or a body fluid, or the preparation forms a gel within a maximum of 15 minutes after introduction in an aqueous medium or a body fluid and disperses or breaks down within a maximum of 30 minutes after said introduction.
WO2014052669A1 Modulation of ire1 Described herein, inter alia, are compositions and methods of using the same for modulating the activity of Ire1.
CN101108192A Phenols glycosides compounds with liveness against osteosporosis The invention relates to the technical field of medical technology, in particular to the application of phenolic glycoside compounds, such as rhizoma curculiginis glucoside, rhizoma curculiginis glucoside B and rhizoma curculiginis glucoside C separated from rhizoma curculiginis in preparing anti-osteoporotic drug. The chemical constitution of the invention is shown in the chart: wherein, R1 indicates-OCH3 or-OH; R2 indicates-H or OH. When R1 is set as-OCH3 and R2 is set as-H, the compound will be rhizoma curculiginis glucoside; when R1 is set as-OH and the R2 is set as-H, the compound will be rhizoma curculiginis glucoside B; when R1 is set as-OCH3 and R2 is set as-OH, the compound will be rhizoma curculiginis glucoside C. After testing, it is proved that the three compounds will outstandingly promote the multiplication of osseus cell, improve activity of alkaline phosphatase, enhance the synthetization of collagen, inhibit the activity of tartrate-resistent acid phosphotase and bone resorption as well as reduce the osseous loss by enhancing the osseous formation and inhibiting the destructive bone resorption. Therefore, the invention, with the activity of resisting osteoporosis, can be applied to prepare the anti-osteoporotic drug.
CN101392014A Bisamidocyanogen androstanes derivates, preparation method and use thereof The invention discloses a diamino etioallocholane derivative, a preparation method and the application thereof. The structure of the derivative is shown as the formula (I) or the formula (II), wherein, R1 or R2 is respectively C1-4 alkyl, C1-4 nitrile group or C1-4 alkynyl independently; R3 is C2-4 alkyl, C1-4 nitrile group or C1-4 alkynyl. Through the determination of activity, the compound has stronger muscle-relaxing action, and the holding time of one-time intravenous thereof is short.
CN1914196B 5- or 6-substituted benzimidazole derivatives as inhibitors of respiratiory syncytial virus replication The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar<2>, R<6>, pyrrolidinyl substituted with R<6>, piperidinyl substituted with R<6> or homopiperidinyl substituted with R<6>, G is a direct bond or optionally substituted C1-10alkanediyl; R<1> is Ar or a monocyclic or bicyclic heterocycle; one of R<2a >and R<2b> is cyanoCl-6alkyl, cyanoC2-6alkenyl, Ar<3>Cl-6alkyl, Het-C1-6alky1, N(R<8a>R<8b>)Cl-6alkyl, Ar<3>C2-6alkenyl, Het-C2-6alkenyl, Ar<3>aminoCl-6alkyl, HetaminoCl-6alkyl, Ar<3>thioC1-6 alkyl, Het-thioC1-6alkyl, Ar<3>sulfonylC1-6 alkyl, HetsulfonylC1-6alkyl, Ar<3>aminocarbonyl, Het-aminocarbonyl, Ar<3>(CH2)naminocarbonyl, Het-(CH2)naminocarbonyl, Ar<3>carbonylamino, Het-carbonylamino, Ar<3>(CH2)ncarbonylamino, Het-(CH2)ncarbonylamino, and the other one of R<2a> and R<2b> is hydrogen; in case R<2a> is hydrogen, then R<3> is hydrogen; in case R<2b >is hydrogen, the R<3> is hydrogen or C1-6alkyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
CA2396156C Osmotic device containing venlafaxine and an anti-psychotic agent The present invention provides an osmotic device containing controlled release venlafaxine in the core in combination with an anti-psychotic agent in a rapid release external coat. A wide range of anti-psychotic agents can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray-coated rather compression-coated onto the device. The device with spray-coated external core is smaller and easier to swallow than the similar device having a compression-coated external coat. The device is useful for the treatment of depression anxiety or psychosis related disorders.
CN101314027A Sea backthern lysine particle The invention relates to a sea buckthorn lysine particle. The sea buckthorn lysine particle is characterized in that sea buckthorn powder, lysine, selenoprotein, zinc gluconate and calcium gluconate are evenly mixed, and the mixture is subject to drying, granulation and sterilization, and thus the sea buckthorn lysine particle is obtained.
CN103006555A Hydroxyethyl starch injection and preparation method thereof The invention relates to a hydroxyethyl starch injection and a preparation method thereof. The hydroxyethyl starch injection is prepared by dissolving hydroxyethyl starch and electrolyte into water for injection; and the content of 5-hydroxymethyl furfural contained in the hydroxyethyl starch injection is alpha, wherein alpha is more than 0 or less than and equal to 1.1 micrograms/milliliter. The preparation method of the hydroxyethyl starch injection comprises the following steps of: (1) taking the water for injection the amount of which account for 50%-60% of the prescription amount, adding the prescription amount of hydroxyethyl starch at a temperature of more than 80 DEG C under the stirring condition, after the hydroxyethyl starch is completely dissolved, adding the prescription amount of sodium chloride or the compound electrolyte, then adding moistened boiled active carbon, boiling, preserving heat for 25-30 minutes, and then cooling to 50-60 DEG C; (2) centrifugalizing and decarburizing liquid medicine cooled to 50-60 DEG C in the step (1), complementally adding the water for injection to full dose, regulating a pH value to 5.5-6.5, carrying out three-level refined filtration on the prepared liquid medicine, and then subpackaging to obtain the hydroxyethyl starch injection. According to the invention, the content of the 5-hydroxymethyl furfural contained in the hydroxyethyl starch injection can be controlled to be less than 1.1 micrograms/milliliter, and therefore the hydroxyethyl starch injection can be more safely and reliably used.
WO2002096905A8 Thiazole compounds useful as inhibitors of protein kinases The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3, Aurora2, and Syk mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatement of various protein kinase mediated disorders.
US20070149555 Prophylatic and/or therapeutic agents for chronic musculoskeletal pain A prophylactic and/or therapeutic agent for diseases accompanied by chronic musculoskeletal pain comprising as an active ingredient a compound having an adenosine A2A receptor antagonistic action, for example, represented by the following formula (I) (wherein R1, R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl, lower alkenyl or lower alkynyl; R4 represents cycloalkyl, —(CH2)n—R5 or the following formula (II); and X1 and X2 are the same or different, each representing an oxygen atom or a sulfur atom) or a pharmaceutically acceptable salt thereof.
CN101543510A Hyperosteogeny medicine The invention relates to a hyperosteogeny medicine which adopts 500 g of 35-40 DEG rice vinegar, 2 to 4 g of iron scurf and 3 to 4 needles; the 3 to 4 needles and the 2 to 4 g of iron scurf are together placed into a bottle containing 500 g of 35-40 DEG rice vinegar, then the bottle is placed at the place of 20-25 DEG C for 6 to 8 months, and metal oxide liquid is generated in the bottle.
CN101721379B Cefuroxime sodium suspension powder injection The invention provides a cefuroxime sodium suspension powder injection. The cefuroxime sodium suspension powder injection comprises the following components by weight part: 1 part of cefuroxime sodium, 2 to 10 parts of surfactant and 3 to 18 parts of lyoprotectants. The cefuroxime sodium suspension powder injection is characterized in that the surfactant is a combination of cholesterol and tween-80 in a weight ratio of 6:1-4:1. The cefuroxime sodium suspension powder injection is prepared unexpectedly by using the emulsification and suspension technologies through specific surfactant after freezing and drying and solves the problem of poor stability of the cefuroxime sodium.
US20080312153 prevention or treatment of disease associated with hyperglycemia: diabetes, impaired glucose tolerance, impaired fasting glycemia, diabetic complications or obesity; e.g. 4-[(4-{3-[1-carbamoyl-1-(methyl)-ethylcarbamoyl]propyl}-2-methylphenyl)methyl]-3-( beta -D-glucopyranosyloxy)-5-isopropyl-1H-pyrazole The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc.; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.
WO2012123506A1 Montelukast intermediate camphorsulfonic salt The present invention is directed to a novel salt of a montelukast intermediate, the process of preparation thereof, the use of such salt in the preparation of sodium montelukast and a process for the preparation of sodium montelukast making use of said salt.
WO2010144685A1 Crystalline forms of febuxostat New forms of Febuxostat have been prepared and characterized. These forms are useful, for example, in the chronic management of hyperuricemia in patients with gout.
CN103641925A Covalent polycompound of water-soluble polysaccharide and taxane compound, and preparation method and medical application of covalent polycompound The invention relates to a covalent polycompound of water-soluble polysaccharide and taxane, and a preparation method and medical application of the covalent polycompound. The method disclosed by the invention comprises the following step: connecting the taxane compound to the water-soluble polysaccharide through a covalent bond by adopting selective protection and selective deprotection methods and a plurality of degradable structure units, so as to obtain the covalent polycompound which can retain the biological activity of the taxane compound and is relatively simplex in structure. The novel covalent polycompound is good in water solubility, and can replace an existing clinical taxane preparation free of a cosolvent with toxic and side effects.
WO2011016472A1 Pyridine and pyrimidine derivatives having ttk-inhibiting activity Disclosed are: an effective inhibitor of TTK protein kinase; and an effective medicinal agent. Specifically disclosed are: a compound; and inventions relating to the compound (e.g., a pharmaceutical composition, a TTK inhibitor, and others). Novel compounds are discovered, each of which can inhibit the activity of TTK kinase and has specific properties particularly useful for the formulation of a medicinal agent that can treat the diseases. Therefore, the compounds are useful for diseases for which the inhibition of the activity of TTK kinase is believed to be effective.
EP1797093B1 Novel 3-methyl-7-butinyl-xanthines, production thereof, and use thereof as medicaments The invention relates to novel substituted xanthines of general formula (I), wherein R1, R2, and X are defined as mentioned in the claims, the tautomers, enantiomers, diastereomers, mixtures, and salts thereof, which have valuable pharmaceutical properties, especially an inhibitive effect on the activity of the dipeptidyl peptidase-IV (DPP-IV) enzyme.
US6991624 Methods and compositions for use in perfusion applications Methods and compositions for use in perfusion applications are provided. In the subject methods, a subject or derivative thereof, e.g. isolated organ or tissue, is infused, perfused and/or transfused with at least two fluid compositions. The first fluid composition is a non-naturally occurring biological buffer free plasma-like solution and the second fluid composition is a fluid blood composition. In a preferred embodiment, an additional volume of the first solution, or a derivative thereof, is administered to the patient following introduction of the fluid blood composition. Also provided are kits and systems for performing the subject methods. The subject methods and compositions find use in variety of perfusion applications, including the treatment of hypothermic surgical applications, cryogenic procedures, and the like.
CN101199820A External sticking plaster for treating hepatitis Disclosed is an emplastrum for external use for treating hepatitis to reach the effect of externally treating internal illness. The proportion by weight of the herbs used in the emplastrum is that: artemisia capillaris thumb of 60 to80 shares, rheum officinale baill of 10 to 30 shares, angelica of 20 to 30 shares, scutellaria of 50 to 60 shares, rhizoma seu radix notopterygii of 20to 30 shares, cape jasmine of 10to 20 shares, rhizoma coptidis of 5 to 10 shares, Rhubarb Root of 6to 10 shares, mirabilite of 20 to 30 shares, calamus of 6 to 10 shares, bupleurum root of 10 to 20 shares, red sage root of 10 to 20 shares, Fructus Toosendan of 10 to 20 shares, peach kernel of 10 to 20 shares, cyperus rotundus l of 10 to 20 shares, Curcuma longa of 10 to 20 shares, new yam of 80 to 120 shares. The emplastrum can relieve the depressed liver, regulate both liver and spleen, promote blood circulation by removing blood stasis and is free of side effect in long term use.
EP1313485B1 Use of an aldosterone receptor antagonist to improve cognitive function Aldosterone receptor antagonists for the prevention and treatment of cognitive dysfunction are disclosed.
WO2009015446A2 Triazole derivatives as viral replication inhibitors The present invention relates to novel compounds and to their use as a medicament, more in particular for the treatment or prevention of viral infections in mammals. The invention also relates to processes for the preparation of compounds according to the invention and to pharmaceutical compositions comprising them.
WO2014140241A1 Pyridine derivatives as dgat-1 inhibitors Described herein are compounds of formula (I): The compounds of formula (I) act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
WO2010038428A1 Alternative agent to taxane anti-cancer agent Disclosed is an alternative agent to a taxane anti-cancer agent such as paclitaxel, which enables the extension of the withdrawal period for the taxane anti-cancer agent while maintaining the therapeutic effect of the taxane anti-cancer agent. The alternative agent comprises a p38MAPK inhibitor. The alternative agent is administered to a patient who has a history of administration of the taxane anti-cancer agent at least two times over a period of 2 to 8 months for the purpose of potentiating an anti-cancer activity of the taxane anti-cancer agent and/or reducing adverse side effects of the taxane anti-cancer agent. During the period of 2 to 8 months, the taxane anti-cancer agent is not administered to the patient.
CN102641276A Compound clobetasol propionate mixed micellar solution and preparation method thereof The invention provides a compound clobetasol propionate mixed micellar solution. Phosphatide and cholate are mainly utilized to prepare the mixed micellar solution which is used for packaging clobetasol propionate and tretinoin. The mixed micelle solution can be simply prepared, and the medicament stability can be guaranteed in the process of preparation. By preparing a mixed micelle system from the phosphatide and the cholate, the problem of medicament dissolution is solved. Compared with a common ointment, the mixed micelle solution has a higher retention volume on skins, and the quantity of the medicament on local skins and the therapeutic index can be increased. The mixed micelle solution can be further prepared into an ointment and a gel, and is mainly used for treating psoriasis vulgaris, dermatitis, eczema, etc.
CN102987092A Feed additive for improving disease resistance of escherichia coli The invention relates to a feed additive for improving disease resistance of escherichia coli. The feed additive is prepared from 18-24 parts of burdock, 15-20 parts of herba patriniae, 15-20 parts of cordate houttuynia, 12-16 parts of folium isatidis, 12-16 parts of radix sophorae flavescentis, 8-12 parts of submerged root rhubarb, and 3-5 parts of gypsum as raw materials. The feed additive disclosed by the invention plays the roles of resisting viruses, clearing heat, diminishing inflammation, detoxifying, invigorating stomach, dehumidifying, breaking through intestines and regulating the flow of vital energy, and also can prevent and treat colibacillosis. Therefore, the recovery rate and the daily gain of piglets are improved, and the mortality of the piglets is reduced.
US20130029902 Cxc chemokine receptor 4 (cxcr4) antagonistic polypeptide A peptide having the following amino acid sequence: Z1-LVRYTKKVPQVSTPTL-Z2(ALB-408) and its biologically active fragments and/or variants and/or derivatives, especially amidated, acetylated, sulfated, phosphorylated and/or glycosylated derivatives, and peptides obtainable by multiple synthesis which have the biological activity of ALB408-423; wherein Z represents number of from 0 to 10 amino acid residues.
US7012138 Chiral polysaccharide esters, one of the methods for preparing them and their uses for obtaining optically enriched acids or for chiral chromatography The present invention relates to chiral esters of polysaccharides, preferably of cellulose, amylose, β-cyclodextrin or amylopectin, obtained by reacting, in basic medium, polysaccharides (polyhydroxylated compounds) with racemic or enriched acid chlorides bearing a hydrogen and an aromatic group on their a carbon. This acid precursor (I) may be α-phenylpropionic acid, ibuprofen, ketoprofen or naproxen and, more generally, any acid derivative which may lead to a reactive form of ketene type. These novel asymmetric esters of polyhydroxylated compounds may be used as means of chiral enrichment, as medicinal systems with sustained and controlled release of enriched chiral active principles, these active principles consisting of the acyl parts of the esters grafted onto the hydroxyls (or even onto the amines) of the polyhydroxylated compounds, or alternatively as chiral stationary phases (CSPs). The invention is also directed toward a process for preparing these esters, to a chiral enrichment process and to the enrichment means, the medicinal systems and the CSPs targeted above.
CN1563007A 9-(2-fatty ester ethoxy methyl) guanine, liposome, and preparation emthod This invention relates the prosome of Axilowei-9-(2-fatty acid ester ethoxy methyl) quanine and its liposome. In said invented product prodn. sodium deoxycholate method is used, with advantages of: simple synthesis method, economic and easy purification, high yield >70%, high pureness >99%, commercialization prodn. And experimental result shows that: said products have strong effect of anti-hepatitis B virus and anti-herpesvirus, better than their mother medicine-Axilowei.
US20110293653 Antagonists of mir-155 for the treatment of inflammatory liver disease Provided herein are methods of treating or preventing an inflammatory liver disease in a subject, such as alcoholic liver disease (ALD), by administering to said subject an miR-155 antagonist.
CN103030620A Drug, food, or cosmetic which has anti-obesity agent and fat accumulation inhibiting action The invention provides an anti-obesity agent and drug, food or cosmetic in which there is no fear of a side effect, which is safe, and has an outstanding fat accumulation inhibiting action. Specifically, the invention relates to the anti-obesity agent includes a new compound A expressed by formula (2), and the drug, food or cosmetic comprising the anti-obesity agent and having the outstanding fat accumulation inhibiting action.
CA2227386C Piperazine derivatives and their use as 5-ht1a antagonists A compound of general formula (A) is described together with pharmaceutically acceptable acid addition salts thereof. The compound a 5-HT1A antagonist which is useful in the treatment of CNS disorders in mammals.
US20090203677 Dual Pharmacophores - PDE4-Muscarinic Antagonistics The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
WO2013107441A1 Process for producing a solid pharmaceutical composition comprising the active ingredient rasagiline The present invention relates to a process for producing a solid pharmaceutical composition comprising the active ingredient rasagiline, comprising: dissolving a pharmaceutically acceptable rasagiline salt in an aqueous solvent to obtain a rasagiline salt solution; admixing a solid carrier with the rasagiline salt solution. In order to provide a process by means of which compositions in which the rasagiline has elevated stability are obtainable and the composition can correspondingly be stored for longer, it is proposed that the pH of the rasagiline salt solution be adjusted to a value of less than 3.5 by means of a pharmaceutically acceptable acid.
CN103479622A Application of Neonectrolide A to in preparation of medicament for treating and preventing renal fibrosis The invention provides an application of Neonectrolide A to in preparation of a medicament for treating or preventing renal fibrosis, and belongs to the technical field of novel applications of medicaments. The application in the invention belongs to a first disclosure. The Neonectrolide A belongs to a brand new matrix type, and has high inhibitory activity on renal fibrosis and the characteristic of outstanding substantiality; meanwhile, the Neonectrolide A is a significant progress in the prevention and treatment of renal fibrosis.
WO2009141079A1 Novel [f-18]-labelled l-glutamic acid and l-glutamine derivatives (ii), use thereof and method for their production The invention relates to compounds and the synthesis of [F-18] labelled L-glutamic acid and [F- 18] labelled L-glutamate, to their derivatives according to formula (I) and to the uses thereof.
WO2013156413A1 Methods of treating lactose intolerance Disclosed herein are methods for treating lactose intolerance, including compounds that may be specific or modulate PPARγ receptors.
WO2009014770A2 Combinations of dopamine d2 receptor blockade with norepinephrine reuptake inhibition and with norepinephrine alpha 2 receptor blockade Methods of treating and or preventing substance abuse/dependence, and alcohol abuse/dependence in particular. Combinations of medications are also disclosed.
EP2137175A1 Novel phenanthrenequinone-based compound and pharmaceutical composition containing the same for the treatment or prevention of disease involving metabolic syndrome Provided is a pharmaceutical composition for the treatment and/or prevention of disease involving metabolic syndromes, comprising (a) a therapeutically effective amount of a particular compound represented by Formula 1 as defined in the specification, or isomer, prodrug, or solvate or thereof, and (b) a pharmaceutically acceptable carrier, a diluent or an excipient, or any combination thereof.
US20080009542 Polymorphic form of fluoro-7-(2,2,2-trifluoroethoxy) phenoxathiin-10,10-dioxide Provided herein is a new form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide, which demonstrates higher stability relative to other forms of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide. In particular, this new form affords less dosage critical administration of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide relative to other forms. The new solid form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide has been determined and is provided herein. This new solid form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide can be characterized by any of a number of its properties, including, but not limited to, melting point, differential scanning calorimetry, infrared spectroscopic spectrum or portions thereof, solubility, methods and conditions under which this form is prepared, and/or precipitated from solution, and, when in crystalline form, the crystalline form can be characterized according to the diffraction pattern or portions thereof
CN101259283A Anti-depression noncovalent complex with high dissolvability and preparation thereof The invention belongs to the non-covalent complex technical field, in particular to an antidepressant non-covalent complex with high solubility and a preparation method thereof. The complex is obtained after the inclusion of Beta-cyclodextrin and a broad-spectrum antidepressant new complex which includes SIPI5838 (C25H29C1N2O2 2HC1 2H2O and SIPI5824 (C28H35C1N2O2 2HC1). The synthesis procedures include that the Beta-cyclodextrin and the antidepressant complex are mixed by the mole ratio of 5 to 1 to 1 to 5; the mixture is put in an incubator for 20-28 hours for the complete reaction at the room temperature and under the condition of pH 5-6; the required non-covalent complex is obtained. A curve fitting method is used for processing data measured by electrospray ionization mass spectrometry to obtain that the formation constant of the non-covalent is about 10<3>. The solubility of the complex SIPI5838 and SIPI5824 respectively rises from 6.5mg/ml and 3.5mg/ml to 12.4mg/ml and 8.3mg/ml after the reaction with the Beta-cyclodextrin.
US20050049212 Eating disorders, cachexia, diabetes mellitus, hypertension, coronary heart disease, hypercholesterolemia, osteoarthritis, gallstones, cancers of the reproductive organs, and sleep apnea; drug screening; diagnosis and therapy; kits; regulates metabolism of triglycerides The present invention discloses Bestrophin homologous proteins regulating the energy homeostasis and the metabolism of triglycerides, and polynucleotides, which identify and encode the proteins disclosed in this invention. The invention also relates to the use of these sequences in the diagnosis, study, prevention, and treatment of diseases and disorders, for example, but not limited to, metabolic diseases such as obesity as well as related disorders such as eating disorder cachexia, diabetes mellitus, hypertension, coronary heart disease, hypercholesterolemia, osteoarthritis, gallstones, cancers of the reproductive organs, and sleep apnea.
CN1968694B An analgesic pharmaceutical composition The present invention relates to a pharmaceutical composition with pain easing function. The analgesic pharmaceutical composition consists of aconitine compound as the effective medicine component, comprising two or three of benzoylmesaconine, mesaconitine and hypaconitine. According to the results of toxicity tests, the LD50 values of mesaconitine and hypaconitine are 6.41mg/kg and 12.8mg/kg respectively, wherein benzoylmesaconine has the relatively lowest toxicity in three and its LD50 value is not measurable and the maximum tolerance dose is 1000mg/kg weight. In accordance with the present invention, two or three aconitine compounds are also capable of proportionally used with best proportioning to achieve better cooperative synergism effect, which has ideal analgetic effect and relatively low toxicity and provides a new clinical choice.
US20080317849 Method for Improving the Medical Treatment of Pain Methods for improving pain management in a mammal, the methods comprising administering a combination of a strontium-containing compound and a second therapeutically and/or prophylactically active substance selected from the group consisting of analgesic agents, anti-inflammatory agents and palliative agents to the mammal. Pharmaceutical compositions for use in such methods, comprising a strontium-containing compound and a second therapeutically and/or prophylactically active substance selected from the group consisting of analgesic agents, anti-inflammatory agents and palliative agents.
CN103655565A Palonosetron medicament composition and preparation method thereof The invention discloses a palonosetron medicament composition for injection. The palonosetron injection consists of palonosetron, acetic acid and sodium calcium edetate. The preparation method comprises the following steps: adding a prescription amount of acetic acid and sodium calcium edetate into injection water, stirring to dissolve, adjusting the pH value, adding palonosetron, stirring till complete dissolving, adding medicinal charcoal, stirring, performing suction filtration, compensating injection water till being full dose, uniformly mixing, finely filtering, filling, sterilizing, inspecting in light and storing in warehouses so as to obtain the palonosetron medicament composition. The palonosetron medicament composition is good in stability, the product yield is improved, the cost is lowered, industrialization is achieved, and the palonosetron medicament composition can be well applied to clinical treatment and has remarkable advantages.
WO2012076934A1 Glycomimetic compounds as anti-infectious against pathogens lectins The present invention relates to a calixarene-based glycosylated compound (I) having the formula : (I) wherein D is independently selected in the group comprising a –CH2 –group, an oxygen atom, a sulphur atom, a sulfinyl group or a sulfonyl group, E is independently selected in the group comprising a hydrogen, an alkyl having from 1 to 10 carbon atoms, an aryl having from 6 to 20 carbon atoms, a nitrogen dioxide group, an azide group, an amino group, a guanidinium group,a halogen atom, a –CH2 R group wherein R is a hydroxyl, a halogen, an amino group, a N(alkyl)2 group, a NH(alkyl) group, or E represents a –CO-R' wherein R' is a hydrogen atom, a hydroxyl group or an amino, B represents a A–C group wherein A is independently selected in the group comprising an oxygen atom, a sulfur atom, a NH group or a (CH2 )i group, i being an integer from 1 to 10, C is independently selected in the group comprising a hydrogen, an alkyl, an alkenyl, an alkynyl, or C is a group of formula (II). The present invention also relates to a pharmaceutical composition characterized in that it comprises the said calixarene-based glycosylated compound (I), in combination with pharmaceutically acceptable carriers or diluents. The present invention also relates to the use of the said calixarene-based glycosylated compound (I) or the said pharmaceutical composition, for the manufacture of a drug intended to prevent or treat bacterial infections from pathogens that use lectins in the first steps of infection.
US20130053338 Use of P2X Purinergic Receptor Agonists to Enhance Insulin Secretion in Pancreatic Beta Cells Pharmaceutical compositions containing P2X purinergic agonists, e.g. P2X3 agonists, for increasing insulin secretion in a subject, methods of use, and methods of screening for related compounds and agents.
US20100034801 Non-Polymeric Compositions for Controlled Drug Delivery The present invention provides a novel liquid composition suitable for in-situ formation of a depot system to deliver a bioactive substance in a controlled manner. The composition of the present invention comprises: (a) a hydrophobic non-polymeric carrier material; (b) a water miscible biocompatible organic solvent that dissolves the hydrophobic non-polymeric material; (c) an ionic complex that is formed between an amphiphilic molecule and a bioactive substance having a net charge at neutral pH in water. The present invention also provides a method of manufacturing and use of the composition thereof.
CN1640410A Helicid capsule agent The present invention discloses a helicid capsule. Said capsule contains helicid effective component and pharmaceutically-acceptable auxiliary agent. Eeach capsule comprises 40-300 mg of helicid, and the described auxiliary agent can be one selected from filling agent, moistening agent, binding agent, disintegrant, lubricating agent, slow-releasing material or control-releasing material or their mixture. Its therapeutic effect is stable and reliable.
US6943016 incubating a mixture of astrocytes and glial cells from patient surgical resection, culturing, astrocytes joining to the culture vessel, removing the un-attached cells; purification; treating CNS trauma, neurodegenerative disorders The invention provides an essentially pure preparation of human adult astrocytes, and a method of producing same. The purified astrocytes are useful for the treatment of neurodegenerative disorders or trauma to the central nervous system.
EP1453846B1 14 or 15 membered macrolides with antibacterial activity The present invention relates to 14 or 15 membered macrolides substitued at the 4" position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
CN1961659A A method for promoting ovary maturity and brooding of blue crab The invention relates to a method for accelerating the oophoron mature and oostegite of green crab, wherein based on the genesis nerve endocrine mechanism of 5-hydroxytryptamine, it uses external hormone to accelerate the oophoron mature and oostegite. And the method comprises that preparing 5- hydroxytryptamine solution while the solvent is disinfected seawater, the contents of 5-hydroxytryptamine and disinfected seawater is 1-2mg:1mL; each crab is injected with 1-3 agents of 5-hydroxytryptamine at 5-15 mug/g, while the injection interval time is 5-10 days. The invention can shorten the oophoron mature period, with low cost.
WO2013189864A1 N-alkyltriazole compounds as lpar antagonists Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis...
WO2009062371A1 Carbamate derivatives, and the use as medicament Carbamate derivatives of 5- or 6-membered ring represented by the general formula (I), a process for preparing them, pharmaceutical compositions comprising them, intermediates for preparing the general formula (I), and a process for preparing the intermediates, and their use as a medicament, especially for cholesterol ester transfer protein (CEPT) inhibitors.
CN101653569B Medicine for curing bladder neoplasm The invention relates to a medicine for curing bladder neoplasm. The medicine is prepared from the following raw materials according to the parts by weight: 4-6 parts of cocklebur fruit, 3-5 parts of magnolia flower, 3-5 parts of bittern product, 6-8 parts of cortex meliae, 10-12 parts of pumpkin seed, 4-6 parts of gemma agrimoniae, 4-6 parts of stone-like omphalia, 6-10 parts of cortex ailanthi,6-8 parts of tuckahoe, 6-8 parts of the root of red-rooted salvia, 4-6 parts of alisma orientale, 2-6 parts of eucommia, 6-8 parts of clove, 6-8 parts of root of herbaceous peony, 10-20 parts of black morning glory, 10-18 parts of euphorbia pekinensis, 10-18 parts of milk vetch, 8-10 parts of rhizoma imperatae, 8-10 parts of honeysuckle, 10-12 parts of the root of red-rooted salvia, 6-8 parts of rhubarb, 6-10 parts of euphorbia kansui, 4-6 parts of plantain seed, 4-6 parts of orange peel and 4-6 parts of green tangerine peel. The beneficial effect of the invention is that the relapse rate is low, the curative effect is good, the side effect is small, the cost is low and the use is convenient without pain.
US20100099705 Argatroban formulation An aqueous, stable, sterile pharmaceutical composition of the thrombin inhibitor argatroban in a solution containing an acid to solubilize the argatroban, substantially free from dehydrated alcohol is described, as well as a method for its preparation.
CN102649788A Beta-L-2'-desoxy-thymin-nucleoside derivative, preparation method and purposes thereof The invention belongs to the technical field of chemical medicines, and particularly relates to a Beta-L-2'-desoxy-thymine nucleoside derivative, a preparation method and purposes thereof. The Beta-L-2'-desoxy-thymine nucleoside derivative has a structure as showed in a format I, wherein R1 and R2 are independent O, S or Se; when one of the R1 and the R2 is O, R3 is halogen, -OH, -NH2, C1-C8 alkyl, (CH2)nF, (CH2)n-1CHF or CF3; R4 is halogen, H, or CF3; and n is 1-8. The invention provides the derivative which has activity of resisting hepatitis virus, and offers a new choice for preparing medicines capable of treating the hepatitis.
WO2009091374A3 Fused heterocyclic derivatives and methods of use as c-met inhibitors Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
CN101607954A Danshensu derivative, preparation method thereof, and application thereof in pharmacy The invention belongs to the field of medicament synthesis, and relates to a Danshensu derivative. The Danshensu derivative with a stable structure as above is obtained by combining Danshensu analogue and nitryl. By culturing primary rat cardiocytes, establishing a hypoxia model of cardiocytes and acute and chronic rat models of myocardial infarction, and performing pharmacological tests in vivo and in vitro, results show that the compound has good effect of protecting hypoxic cardiac muscle and certain anti-HIV activity. The compound can be taken as a pilot compound of original innovative medicaments for resisting myocardial ischemia to further prepare medicaments for treating ischemic heart disease and medicaments with anti-HIV activity.
US20060046966 Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis Peptido and peptidomimetic compounds of the formula: wherein the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also provided.
EP1150707B1 USE OF AN OmpA ENTEROBACTERIUM PROTEIN ASSOCIATED WITH THE ELAGIGILTV PEPTIDE FOR TREATING MELANOMAS The invention concerns the use of an enterobacterium membrane protein OmpA, in particular of Klebsiella pneumoniae, associated with an antigen or a hapten for preparing a pharmaceutical composition designed to generate or enhance a cytotoxic T response directed against a tumor cell. The invention also concerns the use of said compounds for preventing or treating infection or cancer, in particular cancers associated with a tumoral antigen such as melanoma, and pharmaceutical compositions comprising some of said compounds.
CN103354757A Treatment for lipodystrophy The present invention provides a therapeutic compound of formula (I) and their pharmaceutically acceptable salts for the prevention and treatment of lipodystrophy caused because of HIV infection or combination therapy of HIV-1 protease inhibitors (PIs) and/or reverse transcriptase inhibitors (nRTIs) by neutralizing lipohypertrophy, lipoatrophy and metabolic abnormalities in HIV patient.
WO2006080574A1 1,3-dihydro-2h-indole-2-one compound and pyrrolidine-2-one compound fused with aromatic heterocycle It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer’s disease, Parkinson’s disease, Huntington’s chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indole-2-one compound and a pyrrolidine-2-one compound fused with an aromatic heterocycle, which are highly selectively antagonistic to arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable migration into the brain and high concentrations in the plasma, are found out, thereby achieving the above object.
WO2012144661A1 Aromatic heterocyclic derivative having trpv4-inhibiting activity A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I). wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is -C(=0)-NR2- or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.
CN103191122A Antibacterial medicinal composition The invention discloses an antibacterial medicinal composition, consisting of a compound I based on a free acid and a compound II based on a free acid in a weight ratio of (2:1)-(10:1), wherein the quantity of water is 1.0-2.8 percent of the weight of the medicinal composition, the bulk density of the water content is 0.4976-0.7129g/mL. The medicinal composition is good in stability, content uniformity and packaging uniformity, the quality of the medicinal composition is effectively ensured, and the safety of medication is improved.
DE102011007890A1 New fluoroalkyl-substituted pyrazolopyridine compounds are soluble guanylate cyclase stimulators, useful to treat e.g. heart disease, angina pectoris, hypertension, pulmonary hypertension, ischemia, vascular disease or renal insufficiency Fluoroalkyl-substituted pyrazolopyridine compounds (I) are new. Fluoroalkyl-substituted pyrazolopyridine compounds of formula (I) and their N-oxides, salts, solvates, salts of N-oxides and solvates of the N-oxides or their salts are new. A : N or CR3; R3 : H, D, F, difluoromethyl, trifluoromethyl, 1-4C-alkyl, cyclopropyl or cyclobutyl; L : a1-CR4AR4B-(CR5AR5B) p-a2; a1 : point of attachment to the carbonyl group; a2 : point of attachment to the pyrimidine or triazine ring; p : 0-2; either R4A : H, F, 1-4C-alkyl, hydroxy or amino; and R4B : H, F, 1-4C-alkyl (optionally substituted with 1-3 substituents comprising F, trifluoromethyl, hydroxy, hydroxycarbonyl or 1-4C-alkoxycarbonyl), trifluoromethyl, 1-4C-alkoxycarbonylamino or phenyl; or R4A+C+R4B : 3-6 membered carbocycle or 4-6 membered heterocycle (both optionally substituted with 1 or 2 substituents comprising F or 1-4C-alkyl), oxo-group or 2-4C-alkenyl; R5A : H, F, 1-4C-alkyl or hydroxy; R5B : H, F, 1-4C-alkyl or trifluoromethyl; R1 : H or F; R2 : a3-(CR6AR6B) qCF 3; a3 : point of attachment to the pyrazolopyridine; R6A, R6B : H or F; and q : 1-3. Independent claims are included for: (1) the preparation of (I); and (2) a drug comprising (I) in combination with further active agents comprising organic nitrates, nitric oxide donors, cyclic guanosine monophosphate-phosphodiesterase inhibitors, antithrombotic agents, blood pressure lowering agents or lipid modifying agents. [Image] - ACTIVITY : Cardiant; Antianginal; Hypotensive; Respiratory-Gen.; Vasotropic; Nephrotropic; Thrombolytic; Antiinflammatory; Antiarteriosclerotic; Antiarrhythmic; Cardiovascular-Gen.; Antibacterial; Immunosuppressive; Antiallergic; Cerebroprotective; Endocrine-Gen.; Antidiabetic; Antilipemic; Hemostatic; Anorectic; Ophthalmological; Antiulcer; Antianemic; Antiasthmatic; CNS-Gen.; Nootropic; Vulnerary; Neuroprotective; Antiparkinsonian; Anticonvulsant; Neuroleptic; Tranquilizer; Antidepressant; Hypnotic; Antimigraine; Gastrointestinal-Gen.; Dermatological; Cytostatic. - MECHANISM OF ACTION : Soluble guanylate cyclase stimulator. The soluble guanylate cyclase stimulating activity of (I) was tested in a recombinant guanylate cyclase reporter cell line using an in vitro assay. The results showed that 5,5-dimethyl-2-[1-(3,3,4,4,4-pentafluorobutyl)-1H-pyrazolo[3,4-b ]pyridin-3-yl]-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one exhibited a minimal effective concentration of 0.03 mu M.
CN1899306A Use of carbon and carbon containing matter inpreparing medicine for treating human body hemorrhagic syndrome and preparation and preparing method The present invention discloses the application of charcoal and charcoal containing matter in preparing human body hemorrhage treating medicine and the preparation and preparation process. The charcoal is active charcoal or animal or plant charcoal in the grain size of 1 nm to 180 micron; and the charcoal containing matter is charcoal in the grain size of 1 nm to 180 micron and containing hemostatic and antiphlogistic medicine. Owing to the fine size, the preparation of the present invention has greatly raised hemostatic effect.
WO2009076170A2 Combinations of therapeutic agents for treating cancer The invention relates to a combination comprising vascular disrupting agent (VDA), such as 5,6-dimethylxanthenone-4-acetic acid or a pharmaceutically acceptable salt, ester or prodrug thereof; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.
WO2007102074A3 Salts of quetiapine Novel Salts of Quetiapine are disclosed. These salts of the formula (II) wherein S represents an acid selected from the group consisting of benzoic acid, tartaric acid, oxalic acid, p-toluene sulfonic acid, naphthalene sulfonic acid, succinic acid, malic acid, hydrobromic acid; which forms a salt with Quetiapine.
US20080020971 Heptanoic acid derivatives as dipeptidyl peptidase inhibitors The present invention is directed to novel heptanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, particularly in the treatment of type 2 diabetes and conditions that are associated with the same. In addition, the present invention provides pharmaceutical compositions useful in inhibiting DPP-IV enzyme, comprising a therapeutically effective amount of heptanoic acid derivatives. Moreover, the present invention provides a method of inhibiting DPP-IV comprising administering to a mammal in need of such treatment a therapeutically effective amount of a single or a combination of heptanoic acid derivatives of the invention. The invention further relates to the kits and other articles of manufacture for treating disease states associated with DPP-IV enzyme. The invention further relates to a method of identifying a compound that has dipeptidyl peptidase-IV enzyme inhibition activity, comprising following steps: 1. Define the residues of the active site of DPP-IV 2. Define the geometry and force field relationship of the residues identified above in (1) 3. Define the physical parameters of the active site identified in (I) 4. Validate the model based on mutational analysis and in-vitro inhibitor binding studies 5. Screen the library for scaffolds and small molecules that satisfy the model developed in (3) and validated in (4) above. 6. Dock each inhibitor identified in (5) above to the active site of DPP-IV defined in (I). 7. Minimize the energy of the inhibitor and DPP-IV complex using force fields used in (2) above. 8. Compare the energy of interaction of each inhibitor to that of known inhibitors. 9. Synthesize and validate in in-vitro assays
CN101560193A Alpha-polyhalide acetyl piperazinyl oxazolidone compound and antibacterium application thereof The invention provides an oxazolidone compound shown in (I) formula and pharmaceutically acceptable salt thereof, wherein R in the formula is equal to Cl or F; R is equal to H, Cl, and F; X is equal to CH or N; and Y is equal to H or F. The invention also provides a synthesis method of the compound, and the application of the oxazolidone compound used as medicine for treating infectious diseases, especially infectious diseases caused by multi medicament resistant bacteria.
WO2005105082A1 Substituted hexahydro-pyridoindole derivatives as serotonin receptor agonists and antagonists The present application provides novel compounds according to Formula (I): including all stereoisomers, solvates, prodrug esters and pharmaceutically acceptable salt forms thereof, wherein R1, R4a, R5, R6, R7, R8, R9, m, and X are described herein. Additionally, the present application provides novel pharmaceutical compositions comprising at least one compound according to Formula (I). Further, the present application provides methods of treating a patient in need comprising administering a therapeutically effective amount of at least one compound according to Formula (I).
EP2295056A1 Use of SNS-595 for treating leukemia The present invention relates to a compound which is (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid for use in treating a hematologic cancer, wherein the compound is prepared to be administered in a dose of 60 mg/m2- 110 mg/m2.
WO2013141759A3 Use of l-carnosine for the preparation of a nanopreparation having an antihypoxic and antioxidant activity The invention relates to medicine, specifically to neurology and cardiology, namely to the production of a drug in the form of a biologically active nanopreparation having antihypoxic and antioxidant activity. The use of liposomal containers comprising L-carnosine for the preparation of a nanopreparation having antihypoxic and antioxidant activity increases the stability of the L-carnosine and the life thereof in an organism whilst increasing the efficiency of the action of L-carnosine in small doses, as well as extending the range of such drugs. The mentioned use of L-carnosine for the preparation of a nanopreparation having antihypoxic and antioxidant activity comprises a combination of L-carnosine with a combination of substances selected from the group consisting of phospholipids and nonpolar lipids with the following ratio of components, in % by mass: L-carnosine - 1.1 - 1.2; nonpolar lipids such as triglycerides, cholesterol, free fatty acids, DL-α-tocopherol - 1.2 - 2.5; phospholipids such as phosphatidylcholine, phosphatidyl ethanolamine, lysophosphatidylcholine, lysophosphatidyl ethanolamine, sphingomyelin - 95.3 - 96.3. In this application as well, the drug prepared is used to improve tolerance to brain ischemia, to improve recovery after acute hypoxia, and to increase the antioxidant status of brain tissues. Furthermore, the drug is produced in the form of liposomes containing L-carnosine.
EP0888290B1 Azulenyl nitrone spin trapping agents, methods of making and using same The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be colorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g., structural and the like) about the original reactive free radical species.
CN102816198A Preparation method of 3-hydroxy-5-alkenesteroid compounds with ammonia derivative branched chain structure and application thereof in antineoplastic drugs The invention relates to 3-hydroxy-5-alkenesteroid compounds with ammonia derivative branched chain structure, which are 22-nor-3beta-hydroxycholest-5-ene-22-oxime (5a), 22-nor-3beta-hydroxycholest-5-ene-22-semicarbazone and 3-hydroxy-4-ene-pregnane-20-benzyloxyoxime (6), of which the structural formulae are disclosed in the specification. The preparation method comprises the following steps: carrying out 3- hydroxy protection, 5- double bond protection and ozonization reaction on stigmasterol, and carrying out 22- aldehyde functional group conversion to further remove 3- acetyl group, thereby obtaining the 3-hydroxy-5-alkenesteroid compounds 5a and 5b with ammonia derivative branched chain structure. The compound 6 is obtained by directly carrying out one-step reaction on pregnenolone. The experiment proves that the 3-hydroxy-5-alkenesteroid compounds with ammonia derivative branched chain structure have obvious inhibiting action on multiple tumor cell strains, and can be applied to preparation of drugs for treating cancers.
US20100172870 Methods, uses and compositions for modulating replication of hcv through the farnesoid x receptor (fxr) activation or inhibition Uses, methods and compositions for modulating replication of viruses of the Flaviviridae family, such as hepatitis C virus, through the farnesoid X receptor (FXR) activation or inhibition. More specifically, the use of an antagonist of FXR or an inhibitor of expression thereof for the manufacture of a medicament intended for treating a Flaviviridae virus infection in a subject in need thereof. The use of antagonists of FXR, such as guggulsterone, or use of inhibitors of FXR expression. A cell culture system allowing the replication of HCV and to methods for diagnosing HCV infection, screening of anti-viral compounds and vaccine or viral protein production.
CN102018840A Formula for treating summer-heat and damp The invention provides a formula for treating summer-heat and damp. The formula consists of scutellaria baicalensis, rhizoma pinellinae praeparata, almond, honeysuckle, talc, reddish orange, liquorice and indigo naturalis. Every 100 parts of formula comprises 10 to 15 parts of scutellaria baicalensis, 12 to 18 parts of rhizoma pinellinae praeparata, 8 to 12 parts of almond, 8 to 12 parts of honeysuckle, 15 to 20 parts of talc, 5 to 8 parts of reddish orange, 10 to 15 parts of liquorice and 15 to 20 parts of indigo naturalis. The invention has the advantages that: the formula for treating the summer-heat and damp can eliminate the summer heat and damp, and has complete treatment effect.
CN102898522A Tetrahydropyridinopyran-monoclonal antibody CD14 conjugate with anti-tumor activity and preparation method and use thereof The invention discloses tetrahydropyridinopyran-monoclonal antibody CD14 conjugates with anti-tumor activity and a preparation method and use thereof. The structure of the conjugate is represented by a formula (II). Under the action of dicyclohexylcarbodiimide (DCC) serving as a condensing agent, an amino acid residue on the carbon terminal of a CD14 monoclonal molecule is bonded with an amino on a pyran ring in a tetrahydropyridinopyran derivative to form a monoclonal antibody conjugate CD14-TPP of the formula (II). CD14-TPP can effectively inhibit the proliferation of a human erythroleukemia cell line K562, an ovarian cancer cell line MDR-MB-231 and a liver cancer cell line SMMC-7721 with an IC50 value much lower than 5-fluorouracil (5Fu) which is a conventional chemotherapy medicine. The conjugate of the formula (II) with low toxic effect on normal bone narrow cells of mouse can be used for preparing medicines for treating leukemia, ovarian cancer and liver cancer.
WO2008076278A4 Methods of cancer treatment with igf1r inhibitors This invention relates to compositions and methods useful for treating various cancers. Therapeutic combinations and methods of use thereof are also covered in the present application.
CN102772400A Pharmacological use of levistilide A The invention relates to the field of pharmacological science, in particular to a levistilide A or pharmacologically acceptable salt, prodrug and pharmacological use thereof. The levistilide A or the pharmacologically acceptable salt and the prodrug thereof disclosed by the invention can be used to treat liver fibrosis or liver cirrhosis.
CN101167879B Preparation for increasing erection rigidity and prolonging intercourse endurance and condom containing the same The invention relates to a medicament for increasing erectile hardness and prolonging coital persistency, and a condom which contains the medicament. Raw material combination is that 5 to 10g diclothane, 5 to 10g dicaine, 0.04 to 0.1g prostaglandin E1, 5 to 20g laurocapram, 10 to 20g phentolamine mesylate, 10 to 20g secretio bufonis, 25 to 50g cardoverine, 10 to 30g quebrachine, and eight crude medicine such as panax ginseng crude drug, barren wort crude drug, Sichuan aconite root crude drug, and strychnos nux-vomica crude drug and the like. Matrix is silicone oil or carbomer, the eight crudedrugs such as, the panax ginseng crude drug, the barren wort crude drug, the Sichuan aconite root crude drug, and the strychnos nux-vomica crude drug and the like are made into clear paste. The clearpaste is dissolved into the secretio bufonis, the cardoverine, and the quebrachine, and then the clear paste is uniformly stirred with the diclothane, the dicaine, the prostaglandin E1, the phentolamine mesylate, and the laurocapram. Miscible liquids are slowly added into water to make medicament. The medicament is instilled into condoms to make condoms. The invention has 90 percent effective rate to impotence, which has 99 percent effective rate to premature ejaculation patients and to prolong coital time.
WO2008004341A1 α-SUBSTITUTED PHENYLPROPIONIC ACID DERIVATIVES The invention provides α-substituted phenylpropionic acid derivatives functioning as ligands of PPAR's α, δ and γ. α-Substituted phenylpropionic acid derivatives represented by the general formula shown below; pharmaceutically acceptable salts thereof; or hydrates of both: [Chemical formula] wherein R1 is trifluoromethyl, substituted or unsubstituted phenyl, cycloalkyl of 4 to 8 carbon atoms, substituted or unsubstituted adamantyl, carboranyl, or diamantyl; R2 is hydrogen or halogeno; R3 is alkoxy of 1 to 10 carbon atoms or benzyloxy; R4 is lower alkyl of 1 to 6 carbon atoms; and R5 is hydrogen or halogeno.
CN101559228A Pharmaceutical composition for treating chronic stable angina pectoris with hyperlipemia The invention relates to a pharmaceutical composition for treating chronic stable angina pectoris with hyperlipermia, which comprises the components of a drug carrier, a sino atrial node If current selective specificity inhibitor or pharmaceutical salt thereof, and an HMG-CoA reductase selective depressant or pharmaceutical salt thereof; the sino atrial node If current selective specificity inhibitor or the pharmaceutical salt thereof is Ivabradine hydrochloride; and the contents of the components of the medical composition by mass unit are 2.5 to 10 of the sino atrial node If current selective specificity inhibitor and 2.5 to 100 of the HMG-CoA reductase selective depressant. The medical composition has good synergistic effect when treating the chronic stable angina pectoris with the hyperlipermia, and has good effect of lowering hyperlipemia for hyperlipoidemia and hemorheology effect.
US20110224250 Isoquinoline derivative, and pde inhibitor comprising same as active ingredient The present invention provides a novel isoquinoline derivative which is useful as a pharmaceutical agent having a phosphodiesterase inhibitory activity. The isoquinoline derivative of the present invention is represented by the following general formula (1):
CA2190377C Use of topical treatment compositions comprising alpha hydroxy acid in the treatment of striae distensae A method is provided to treat and or prevent striae distensae lesions by topically applying to the skin affected with the lesions an effective amount of a treatment composition containing an alpha hydroxy acid, such as glycolic acid, preferably by daily application in a pharmaceutically acceptable vehicle, such as a cream base, at a concentration of from 2 to 30 percent by weight. When applied during the striae rubrae stage, the alpha hydroxy acid may be effective to prevent the formation of striae albae lesions, and when applied in either stage, the alpha hydroxy acid may be effective to reduce the width and depth of the lesions, and improve the color of striae rubrae.
CN101781330A Propofol, phosphate and amino acid double salt and preparation method and application thereof The invention discloses propofol, phosphate and amino acid double salt and a preparation method and application thereof. The method comprises the following steps of: reacting propofol as a raw material with a phosphorylating reagent under a basic condition to obtain a phosphorus oxychloride intermediate; hydrolyzing the phosphorus oxychloride intermediate to obtain propofol ethyl phosphoric acid;then salifying with basic amino acid and concentrating to obtain a crude product; and recrystallizing and purifying the crude product to obtain the propofol, phosphate and amino acid double salt witha structure formula shown as (1), wherein R is the basic amino acid. The medical double salt has favorable water solubility and stability and can be prepared into injections, oral solutions, capsules, tablets and the like after mixing with necessary auxiliary materials. The invention obviously improves the water solubility and the bioavailability of the propofol, reduces irritation and increases therapeutic cooperativity. The synthesis method has the advantages of simple operation, easy obtainment of the raw material, low cost and high yield.
US20100113373 Antiviral supplement formulations The disclosure provides an oral antiviral supplement composition comprising a lysine, an ascorbic compound, a flavonoid glycoside, a threonine, and a pyridoxine. The disclosure also provides a method of reducing viral replication in a cell comprising treating a virus-infected cell with a composition of the disclosure. The disclosure further provides a method for the treatment and prophylaxis of a viral infection in a patient comprising administering a composition of the disclosure.
US7151101 For prevention/treatment of cancer, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, viral diseases and neurodegenerative diseases The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention relates to compounds having the formula: or pharmaceutically acceptable salts thereof, wherein R1, Q1, Q2, and X are as described in the specification. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment end prevention of various disorders.
US20090215908 Toll like receptor (tlr) signaling antagonist The present invention relates to novel synthetic toll like receptor antagonist. The present invention in particular provides compounds, methods and compositions for specifically inhibiting immune stimulation involving TLR ligands, especially TLR-4. The compounds are potentially useful in treatment of inflammation, autoimmunity, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.
US6936285 Use of Ginkgo biloba extracts for preparing a medicine The invention relates to the use of Ginkgo biloba extracts for preparing a medicament intended to ease the withdrawal of individuals dependent on the consumption of a substance engendering dependency and/or addiction, such as in particular alcohol, amphetamines, tobacco, drugs inducing toxicomania.
WO2009004060A1 Novel triazine compounds for treatment of cancer The present invention relates to novel triazine compounds, to processes for preparing them, to a pharmaceutical composition comprising them, and to the use thereof for the treatment of human cancers. The novel triazine compounds are notable, compared to the known triazine compounds, for improved efficacy with simultaneously reduced toxicity, i.e. for lower side effects.
US7741312 Benzylaminosulfonic Acid or portion or analogue linked to a carbohydrate or glycomimetic for modulating processes mediated by selectin binding such as autoimmune and inflammatory diseases, shock and reperfusion injuries Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids, which include a portion or analogue thereof linked to a carbohydrate or glycomimetic.
CN103261194A Oxazolyl-methylether derivatives as ALX receptor agonists The invention relates to oxazolyl-methylether derivatives of formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
US20080293785 Substituted benzothiazole kinase inhibitors The present invention is directed to substituted benzothiazole compounds of formula (I): and forms thereof, their synthesis and use for treating a chronic or acute protein kinase mediated disease, disorder or condition.
US20120328619 Trispecific Therapeutics Against Acute Myeloid Leukaemia The present invention relates to a molecule having binding specificities for (a) CD123; (b) CD16 and (c) CD33. The present invention further relates to the molecule of the invention, wherein the molecule comprises a first immunoglobulin domain comprising a VL domain linked to a VH domain, wherein the immunoglobulin domain specifically binds to CD123; a second immunoglobulin domain comprising a VL domain linked to a VH domain, wherein the immunoglobulin domain specifically binds to CD16; and a third immunoglobulin domain comprising a VL domain linked to a VH domain, wherein the immunoglobulin domain specifically binds to CD33. The present invention furthermore relates to a nucleic acid molecule encoding the molecule of the invention. In addition, the present invention relates to diagnostic and pharmaceutical compositions and the use of the molecule or the nucleic acid molecule of the invention in the treatment of acute myeloid leukaemia and/or myelodysplastic syndrome.
EP2654746A1 Antibacterial or anti-acne formulations containing usnic acid or an usnate and a metal salt An antibacterial or anti-acne formulation suitable for topical or local application to human skin containing (a) either usnic acid or an usnate and (b) a metal salt selected from copper salts, bismuth salts, and mixtures thereof, wherein if the component (a) is an usnate, the components (a) and (b) are not the same compound.
CN102613453A Marine organism type enteral nutrition preparation for diabetes patients, preparation method of marine organism type enteral nutrition preparation and application The invention discloses a marine organism type enteral nutrition preparation for diabetes patients, a preparation method of the marine organism type enteral nutrition preparation and application. The nutrition preparation includes, by weight, from 3 to 15 parts of algal polysaccharides, from 1 to 5 parts of marine edible animal protein peptide powder, from 3 to 5 parts of microalgae oil, from 0.3to 2 parts of spirulina powder, from0.1 to 1 part of taurine, from 40 to 45 parts of balsam pear polysaccharide or pumpkin polysaccharide, from 10 to 15 parts of soybean protein isolate powder, from 7 to 10 parts of medium chain triglyceride, from 3 to 8 parts of konjac dietary fibers, from 1 to 5 parts of fruit and vegetable powder, from 0.1 to 0.5 part of wheat bran, from 0.1 to 0.5 part of alpha-lipoic acid and a trace of trace element additives. Marine active functional matters with unique pharmacologic bioactivity are reasonably compounded according to needs of nutrition and metabolism of the diabetes patients, and the personal enteral nutrition preparation for the diabetes patients is developed, provides balanced nutrition for the diabetes patients and former diabetes patients, effectively relieves malnutrition, prevents diabetes, assists in regulating blood sugar level, can effectively prevent diabetes complications, and is favorable for increasing the quality of life of the patients and promoting rehabilitation.
WO2012012307A1 Sulfonyl compounds which modulate the cb2 rece Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
CN101823956A Diisopropylamine fenofibrate, preparation method of same, medicinal composition and use of same The invention discloses a diisopropylamine fenofibrate, a preparation method of the same, a medicinal composition and use of the same, relating to the field of medicaments for lowering blood fat and treating fatty liver. The problems that fenofibric acid products is poor in water solubility, has toxic and side effects and the like in the prior art are solved. A product of the invention is obtained through the following steps of: adding a fenofibric acid and diisopropylamine into a solvent, heating to 35-70 DEG C, cooling, separating out a solid, pumping a filtrate, washing the solid with ether, and drying to obtain a white solid which is the diisopropylamine fenofibrate. A diisopropylamine part in the invention can overcome the side effect that the fenofibric acid is heated to be converted into ammonia enzyme and blood sugar and exerts a synergetic effect of lowering the blood fat together with fenofibrate.
CN101797242A Application of cysteamine in preparing medicine for treating cancer The invention discloses application of cysteamine in preparing a medicine for treating cancer. Sensitivity on cancer cells by chemotherapeutics is increased by the cysteamine with low dosage, thereby realizing that cancer cells are effectively killed by the chemotherapeutics with low dosage. The invention greatly improves the medicine effect of the chemotherapeutics and lowers the side effects of chemotherapy.
WO2009127251A1 Combinations comprising a renin inhibitor The invention relates to drug combinations comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof with specific cardiovascular treatment agents of complementary pharmacological mechanism to generate a synergistic therapeutic effect.
WO2009049490A1 Use of aminoglycoside antibiotic in the preparation of pharmaceutical composition for treating drug-resistant bacterial infection The use of 2'-NH2-3',4'-dideoxy--1-N-acylated derivatives of aminoglycoside antibiotic in the preparation of pharmaceutical composition for treating drug-resistant bacterial infection, the preparation of the derivatives and the formulation thereof.
CN102657617A Hot-melt extruded quick release preparation of nimesulide and hot-melt extruding method thereof The invention belongs to the field of pharmacy and relates to a hot-melt extruded quick release preparation of nimesulide and a hot-melt extruding method thereof. The hot-melt extruded quick release preparation is mainly characterized in that copovidone (PVP-VA64, Kollidon VA64) or povidone (PVPK30) serves as a main dispersing carrier material, and when necessary, a sugar alcohol auxiliary material serving as a plasticizer is added into the main dispersing carrier material, so that the aims of reducing extruding temperature and simplifying an extruding process are fulfilled. And due to the adoption of a nimesulide solid dispersion, the hot-melt extruded quick release preparation has the characteristic of quick dissolution.
CN1634064A Itraconazole structurization emulsion composition and its preparing method The invention discloses an itraconazole structurization emulsion composition and its preparing method, characterized in that is a kind of cooperative composition, which comprises itraconazol, triglyceride, tension conditioning agent and water. The composition has the advantages of continuous release and smaller toxic and side actions.
WO2013026547A1 Rotigotine in the treatment of hemispatial neglect and other deficits following stroke The present invention relates to the use of rotigotine for the effective treatment of a condition or disorder selected from neglect, stroke, conditions associated with stroke and/or following stroke. The invention also relates to a rotigotine-containing pharmaceutical composition, like a transepicutaneous pharmaceutical composition especially in the form of a transdermal therapeutic System (TTS).
CN102091314B Composition of dried ginger and evodia rutaecarpa, preparation method thereof and application thereof in preparing attenuating synergistic medicament in radiotherapy and chemotherapy of cancer The invention relates to a natural pharmaceutical composition, a preparation method thereof and an application thereof in preparing an attenuating synergistic medicament in radiotherapy and chemotherapy of cancer. The natural pharmaceutical composition is composed of concentrated extract of decoctions of dried ginger and evodia rutaecarpa, gingerol, evodia rutaecarpa extract and evodiamine in proportion of (1-4):(3-7):(2-9):(2-3). The composition provided by the invention has good curative effects on vomit and the like caused by the side effects of radiotherapy and chemotherapy of cancer, andalso plays an effect on inhibiting tumor.
CN101829099A Application of 4-cinnamoyl chloride silybin in preparing medicaments for treating viral hepatitis B The invention relates to application of 4-cinnamoyl chloride silybin in preparing medicaments for treating viral hepatitis B, in particular to application of 4-cinnamoyl chloride substituted silybin ester type flavonolignan or a pharmaceutically acceptable salt thereof in preparing medicaments for suppressing HBV (Hepatitis B Virus) DNA replication and treating HBV infection diseases. The flavonolignan has definite activity on suppressing the HBV DNA, and the suppression activity on the replication of the HBV DNA under a high dose approaches that of alpha-interferon under a highest concentration of 10,000 units/milliliter, thus the flavonolignan belongs to effective non-nucleoside natural products for resisting the HBV. The pharmacodynamical results indicate that the flavonolignan or the pharmaceutically acceptable salt thereof can be expected to be used for preparing the medicaments for suppressing the HBV DNA replication and treating the HBV infection diseases.
WO2004098579A3 Combination of a glycine/nmda antagonist and a tachykinin nk-1 receptor antagonist for use in the treatment of neurodegeneration The present invention relates to a pharmaceutical formulation comprising a compound which is active as an antagonist of the strychnine-insensitive glycine modulatory site of the N-methyl-D-asparate (NMDA) receptor in combination with a tachykinin NK-1 receptor antagonist, for use in the treatment of neurodegeneration arising, in particular, from stroke or cerebral ischemia.
WO2012092157A3 Nutritional formulations including human milk oligosaccharides and long chain polyunsaturated polyunsaturated fatty acids and uses thereof Disclosed are nutritional compositions including human milk oligosaccharides in combination with long chain polyunsaturated fatty acids and/or carotenoids that can be administered to preterm infants, term infants, toddlers, and children for reducing inflammation and the incidence of inflammatory diseases.
CN101011565A Health food with oxidation resistance and compact bone substance density intensification functions The invention discloses a health food having the effects of oxidation resistance and increasing compact bone substance density, wherein the raw materials include chondroitin sulfate 250-280 parts, soybean isoflavones 15-25 parts, mussel 0.5-0.8 part, sea-tangle 2-3 parts, fish oil 2-4 parts, chitosan 2-4 parts, curcuma longa 2-4 parts, pepper 0.2-0.3 part and aloe 2-4 parts.
US20100280012 Azaazulene compounds An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).
WO2011113798A3 Inhibitors of semicarabazide - sensitive amine oxidase Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase wherein R1, A, X and R2 are as defined in the claims.
CN1626244A Combination for treating skin disease A composition for treating the dermatopathy caused by fungus is prepared from the antifungal medicine and rivanol. Its advantages are higher curative effect, short course of treatment and no recurrence.
WO2012016314A9 Arachidonic acid-derived coxib analogue-substituted compounds for use in treating pain The present invention describes the production of arachidonic acid-derived coxib analogue-substituted compounds and salts thereof for use in treating pain. Furthermore, the invention relates to pharmaceutical compositions containing arachidonic acid-derived coxib analogue-substituted compounds, salts thereof and pharmaceutically acceptable excipients for use in treating pain. The painkillers comprised by the invention can be used alone or in combination with other painkillers, for relieving slight, moderate or severe pain.
US20100093740 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
CA2818361A1 3'-deutero-pomalidomide The present application describes 3'-deutero-pomalidomide, deuterated derivatives thereof, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN102579388A Production of mesalazine colon-specific drug administration sustained-release tablet The invention discloses a production of a mesalazine colon-specific drug administration sustained-release tablet. The mesalazine (5-ASA) is widely applied clinically, and becomes a priority drug for treating inflammatory bowel diseases. The mesalazine is ineffective when being orally taken, because the mesalazine is quickly absorbed in the small intestine, then acetylated and discharged along with urine, thus being not able to reach the colon part. 5-ASA can only play the treatment function when reaches the colon lesion part in a prototype, and is produced into a pH-dependent colon-specific drug administration sustained-release tablet, so that the 5-ASA drug which reaches the colon has enough concentration to have an anti-inflammatory effect. Eudragit L100 and Eudragit S100 can be used to produce a film coating which meets the colon-specific release requirement according to a certain proportion. The mesalazine is produced into a coating sustained-release tablet, so that the 5-ASA drug which reaches the colon has enough concentration to achieve the anti-inflammatory effect.
CN102008573A Quality detection method of oral liquid for clearing lung-heat, relieving cough and preventing asthma The invention provides a quality detection method of oral liquid for clearing lung-heat, relieving cough and preventing asthma. The method comprises the following steps: by means of optimization of chromatographic conditions and tests for preparation methods of a sample and a reference substance, establishing a high performance liquid chromatography (HPLC) for the content of the main effective ingredient-ephedrine hydrochloride in the preparation; and by optimization of a chromatographic separation system, adjustment of proportion of a developing agent and selection of a silica gel plate, a color-developing agent and color-developing conditions, establishing a thin-layer chromatography identification method for Chinese ephedra, licorice and mulberry leaf in the preparation. Methodology experimental study proves that the established methods have the advantages of high accuracy, strong specificity and good repeatability; and qualitative identification and quantitative control of effective ingredients in the preparation are carried out, thus ensuring the stability of the effective ingredients and being beneficial to quality control during the production process.
US7393951 antisense to a nucleotide sequence of positions 47 to 51 of 7SL RNA of the signal recognition particle (SRP); inhibitor of cancer cell growth An antisense oligonucleotide having anti-carcinogenicity, for example, an inhibitory action on growth of cancer cells and a therapeutic or prophylactic action on cancer and the like, as well as an inhibitor of cancer cell growth and a therapeutic or prophylactic agent for cancer, which comprise the antisense oligonucleotide are provided. An antisense oligonucleotide to a nucleotide sequence of positions 47 to 51 of 7SL RNA of the signal recognition particle (SRP), an inhibitor of cancer cell growth comprising the antisense oligonucleotide, and a therapeutic or prophylactic agent for cancer comprising the antisense oligonucleotide.
EP2231609A1 Novel 2-ethyl-methyl-amino-3-amido-6-amino-pyridine derivatives useful as potassium channel activators This invention relates to novel 2-ethyl-methyl-amino-3-amido-6-amino-pyhdine derivatives having medical utility, to use of the 2-ethyl-methyl-amino-3-amido-6-amino- pyridine derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2-ethyl-methyl-amino-3-amido-6-amino- pyridine derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.
CN103142467A Calcitriol ointment and preparation method thereof The invention relates to calcitriol ointment and a preparation method thereof. The ointment is prepared from the following ingredients in percentage by weight: 0.0005% of calcitriol, 0.7-1.2% of meglumine, 25-35% of polyethylene glycol 400, 1.5-2.5% of polyethylene glycol 6000, 50-70% of thickener, 3.0% of humectant and an appropriate amount of antioxidant. According to the ointment, the content of calcitriol is remarkably increased, so that the drug dosage is reduced; and the stability of calcitriol to light and air is improved, and the bioavailability of calcitriol is also remarkably improved.
CN101549160A Application of the sulfur-butyl ether-belta-cyclodextrin in eyedrops of chloramphenicol and method thereof The present invention is application of the sulfur-butyl ether-belta-cyclodextrin in eyedrops of chloramphenicol and method thereof. Adding sulfur-butyl ether -belta-cyclodextrin into formula of the eyedrops of chloramphenicol, the addition is 10-80 g/L. The invention finds SBE-belta-CD (sulfur-butyl ether -belta-cyclodextrin) for improving stability of the eyedrops of chloramphenicol by a series of experiments, capable of improving dissolvability of the chloramphenicol for six times, and because of inclusion of the cavity structure to chloramphenicol, blocking chloramphenicol hydrolysis reaction catalyzed by various ions in solution effectively, degradation of the chloramphenicol in aqueous solution is greatly relieved, by experiments, accelerating for six months and normal temperature storing for 24 months, every index of the chloramphenicol eyedrops still conforms to request of the standard, content of chloramphenicol glycol is less than 8%, content of methyl aldehyde is 0, so stability of the chloramphenicol eyedrops is greatly improved.
WO2012038850A8 Pyrimidones for treatment of potassium channel related diseases The present invention relates to compounds of Formula I as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogenital disorders, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.
EP1958521A1 Method of improving absorbability of epigallocatechin, food, drink and food/drink material using the same and method of producing the same Provided are a food, a drink and a food/drink material having improved EGCg absorabability, and a method of producing the same, by improving the absorbability of EGCg to be taken in. The contents of caffeine and/or epigallocatechin gallate are regulated so that the ratio by mass of caffeine to epigallocatechin gallate contained in a food, drink, food/drink material or oral ingesta comes close to 0.4.
CN102949384A Application of coffee acid 3, 4-dihydroxy benzene ethyl ester to preparation of antitumor drug The invention provides application of a coffee acid 3, 4-dihydroxy benzene ethyl ester to preparation of antitumor drugs. The tumors comprise myeloma, esophagus cancer and ENT tumors; the myeloma comprises single myeloma and multiple myeloma; and the ENT tumors comprise oral cavity cancer and nasal cancer. In vitro tumor model proves that the coffee acid 3, 4-dihydroxy benzene ethyl ester has obvious anti-tumor effect on myeloma, esophagus cancer and ENT tumors; therefore, the invention provides effective drug for prevention and treatment of myeloma, esophagus cancer and ENT tumors.
CN103232395A Sodium ozagrel compound, preparation method and drug composition thereof The invention relates to a sodium ozagrel compound and a preparation method thereof. The structural formula of the sodium ozagrel compound is shown in the formula I in the specification. The invention also relates to a drug composition of the sodium ozagrel compound and a preparation method thereof. The dosage forms of the drug composition include freeze-dried powder injection, small-volume injection or large-volume injection. The sodium ozagrel compound has high purity and the preparations of the sodium ozagrel compound have good stability and are suitable for clinical application.
US20110129469 Methods for treating fatty liver disease In certain aspects, the present invention provides compositions and methods for treating fatty liver disease by administering an antagonist of an ActRIIB signaling pathway. Examples of such antagonists include ActRIIB polypeptides, anti-ActRIIB antibodies, anti-myostatin antibodies, anti-GDF3 antibodies and anti-activin A or B antibodies. A variety of hepatic and metabolic disorders may be improved by treating fatty liver disease.
EP1572672B1 Benzoxazocines and their use as monoamine-reuptake inhibitors Compounds of the general formula (1), wherein one of W, X, Y and Z is N or CR4 and the others are each CH; and R4 is a specified substituent. These compounds inhibit monoamine reuptake, and are useful in the treatment of pain, emesis depression, post traumatic stress disorders, attention deficit disorders, obsessive compulsive disorders, pre-menstrual syndrome, substance abuse and sexual dysfunction.
US20130189314 Enteric-coated ht-2157 compositions and methods of their use Drug compositions comprising the compound HT-2157 and their therapeutic uses, including the treatment of CNS disorders and cognitive impairments and the modulation of cognitive function, are disclosed. More particularly, the present invention relates to enteric-coated formulations comprising HT-2157 that reduce the appearance of clinically relevant methemoglobinemia relative to administration of non-enteric-coated formulations comprising HT-2157.
CN103599121A Application of engeletin in preparation of drug for treating or preventing diabetes pathogenic stroke The invention provides novel application of engeletin in drugs, and particularly relates to application of engeletin in preparation of a drug for treating or preventing diabetes pathogenic stroke. According to the application, 25 to 1000mg of engeletin is adopted, and 25 to 500mg is preferable. Engeletin is in a form of tablet, pill, granules, capsule, syrup, soft capsule and other forms, and the forms of capsule and tablet are preferable.
EP2766380A1 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof Provided herein are 3,3-disubstituted 19-nor- steroidal compounds according to Formula (I) and (III): where R1,R2, R3, R3', R4, R6a, R6a, R11a, and R11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, insomnia, anxiety, depression, traumatic brain injury (TBI), stress, and epilepsy.
CN102988997A Drug-loaded nano particles, preparation method and application The invention provides drug-loaded nano particles, a preparation method and an application, the drug-loaded nano particles comprise a carrier and a drug loaded on the carrier, wherein the drug is the water-soluble drug, the carrier is a chitosan-aliphatic polyester-phosphatidyl ethanolamine graft polymer having a structure shown in a formula (I). The drug-loaded nano particles can control drug release and reduce toxic and side effects of antitumor drugs, and provide the possibility for treating targeted low toxicity of the cancer.
CN102379879A Liranaftate and mometasone furoate containing locally applied compound pharmaceutical composition The invention relates to the technical field of antimycotic medicaments, specifically to a liranaftate and mometasone furoate containing locally applied compound pharmaceutical composition, which contains one or more acceptable auxiliary materials for local application. The invention is characterized in that the weight ratio of liranaftate to mometasone furoate is 1:80-80:1; the balance contains matrix auxiliary materials; The pharmaceutical composition can be emulsifiable paste or ointment, gelata, a solution or an emulsion or a suspension, a coating agent, aerosol or a spraying agent or spray-film, a foaming agent and patch. With the application of the liranaftate and mometasone furoate compound pharmaceutical composition, as mometasone furoate has a vasoconstriction effect, the transdermal absorption rate of liranaftate slows down, local skin tissue concentration of liranaftate is increased, the medicament is minimized to penetrate through the skin into blood, and local skin concentration of the antimycotic medicament is maintained for a longer time.
CN1660079A Antibacterial agent use for fishery and processing technique An antibacterial medicine for preventing and treating the he morrhagic septicemia of fresh water fish is prepared from florfenicol, VC and starch.
EP1305031B1 Combination preparations of 3-n-formylhydroxylaminopropyl phosphonic acid derivatives or 3-n-acetylhydroxylaminopropyl phosphonic acid derivatives combined with specific pharmaceutical active agents The invention relates to pharmaceutical combination preparations for use in the therapeutical and prophylactic treatment of bacterial and parasitic infections, especially malaria. The inventive preparations contain as the active substances 3-N-formylhydroxylaminopropyl phosphonic acid derivatives or 3-N-acetylhydroxylaminopropyl phosphonic acid derivatives combined with other pharmaceutical active agents.
CN102423249A Medical nursing wet tissue with functions of deodorizing and preventing bedsore and preparation method thereof The invention discloses a medical nursing wet tissue with functions of deodorizing and preventing bedsore and a preparation method thereof. The medical nursing wet tissue consists of non-woven fabric soaking solution, wherein the solution comprises main components such as dimethicone copolyol, natural polysaccharide alginate, N-sodium lauroyl sarcosinate and bisabolol. The medical nursing wet tissue disclosed by the invention can be used for daily cleaning care of patients bedridden for a long term and can be used for effectively sterilizing and removing stains, preventing the bedsore, relieving pains of the patients, accelerating the healing of wounds and reducing the possibility of infection and deterioration of the wounds. In addition, the medical nursing wet tissue containing plant type grain amino acid extract which can be used for removing off flavor and purifying air. Meanwhile, the medical nursing wet tissue disclosed by the invention can be heated by microwave so as to ensurethat the patients can enjoy warm servers even if in cold winter.
US20120237443 Functionalizing implantable devices with a poly (diol citrate) polymer The present invention is directed to a novel poly (diol citrates)-based coating for implantable devices. More specifically, the specification describes methods and compositions for making and using implantable devices coated with citric acid copolymers or citric acid copolymers impregnated with therapeutic compositions and/or cells.
EP2217275A2 Pharmaceutical compositon for cleansing of the bowel A pharmaceutical composition comprising a docusate; an osmotic laxative; and a benzoate.
CN102895184A Epirubicin hydrochloride injection The invention provides a new epirubicin hydrochloride injection which has the characteristics of being stable in quality, low in content of related substances and simple in technology.
EP2344126A1 Method for treatment of copd and other pulmonary diseases A method for treatment of patients with pulmonary diseases by providing an aerosolized combination of a methylxanthine and a topical steroid administered into a patient's conducting and central airways. The method utilizes a specific treatment protocol and a nebulizing system providing an aerosol having particles of a predetermined mass medial aerodynamic diameter (MMAD) delivered to the conducting and central lungs with overpressure and under controlled conditions.
CN101766822A Piroxicam beta-cyclodextrin inclusion compounds and preparation method of tablets thereof The invention relates to piroxicam beta-cyclodextrin inclusion compounds and a preparation method of tablets thereof. The preparation method comprises the following steps of: after keeping an alkaline aqueous solution (the pH value is 8.0-11.0) of a component at the temperature of 70-80 DEG C for 1-3 hours, spraying and drying the alkaline aqueous solution at the temperature of 70-80 DEG C and drying in vacuum. Compared with the product obtained by using the method in the prior art, the appearance of the obtained product and the properties of the technology using the product for producing preparations are obviously improved, and the product provides superior conditions for preparing oral-administration preparations.
EP2363397A1 Novel useful therapeutic agent for lower urinary tract symptom Provided is a therapeutic agent for lower urinary tract symptom consisting of (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof or a combination of (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof and a compound selected from the group consisting of α1-adrenergic receptor blockers, 5-α reductase inhibitors, antiandrogen drugs, β3-adrenergic receptor agonists, phosphodiesterase V inhibitors, plant preparations, amino acid preparations, herbal medicines and the like. Also provided is a method of using in combination the above-described therapeutic agent and a surgical treatment such as bladder distention or surgery.
US20110245251 Modulators of the prostacyclin (pgi2) receptor useful for the treatment of disorders related thereto Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).
CA2584747A1 Treatment of osteoarthritis and dosing regimen for arzoxifene The present invention provides a method for treating osteoarthritis in a mammal, comprising administering to a mammal in need thereof, an effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt or solvate thereof.
US20090143470 Invisible Antimicrobial Glove and Hand Antiseptic An alcohol based hand surgical scrub, which includes cationic anti-microbial agent preservatives, cationic polymer film-forming agents and a skin emollient, and provides a long term residual, anti-microbial “invisible glove” on the skin. The composition provides an immediate reduction in bacterial microbes. The polymer system creates an invisible film on the skin following solvent evaporation. This invisible film provides a lasting anti-microbial barrier on the skin which acts to prevent microbial growth.
CA2729656A1 Imidazopyrimidinones and uses thereof The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject compris-ing administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.
WO2014057414A1 Ketamine derivatives The present invention relates to ketamine derivatives of the formula (I), pharmaceutical compositions comprising them, and methods for treating pain comprising administering them, and their use in the manufacture of medicaments for treating pain. The present invention also relates to methods for anaesthetizing and methods for sedating a subject comprising administering ketamine derivatives of the formula (II).
CA2271126C Method of treating bronchitis with uridine triphosphates and related compounds A method of promoting clearance of retained mucous secretions in the bronchi, bronchioles and small terminal airways of a subject in need of such treatment is disclosed. The method comprises administering to the bronchi of the subject a uridine phosphate such as uridine 5'~triphosphate (UTP), or P1,P4-di(uridine-5~) tetraphosphate (U2P4), an analog of UTP, or any other analog, in an amount effective to promote mucociliary clearance and/or cough clearance of retained fluid in the bronchi, bronchioles and small terminal airways. Methods of administering the same would include; aerosol inhalation, any liquid suspension (including nasal drops or spray), oral form (liquid or pill), injected, intra-operative instillation or suppository form.
DE4245089B4 Oral pharmaceutical compsn. for treating hyperlipoproteinaemia or atherosclerosis - comprises hydroxymethyl glutaryl coenzyme A reductase cholesterol inhibitor The compsn. (I) comprises HMG-CoA cpd. of formula R-X-CH(OH)-CH2-CH(OH)-CH2-COOM (II) and an alkaline medium (III) imparting pH of at least 8 to an aq. soln. or dispersion. R = organic radical; X = -CH=CH-; and M = physiologically acceptable cation. (II) is pref. associated with carbonate(s) e.g. a mixt. of (i) water soluble and (ii) water insol. or sparingly soluble carbonates in a ratio of (i) to (ii) of 1.4-2:1. (II) is pref. fluvastatin sodium and (i) is pref. caclium carbonate and (ii) is pref. Na (bi)carbonate. (I) pref. comprises 0.5-60 wt.% (II), 0.5-40 wt.% Ca carbonate, 0.5-20 wt.,% Na bicarbonate and 10-65 wt.% microcystalline cellulose.
CN1903206A Alprostadil freeze-dried emulsion and its prepn. method A freeze-dried emulsion of prostaglandin El contains proportionally prostaglandin El, the oil for injection, emulsifier, stabilizer, and freeze-drying protector. Its preparing process is also disclosed.
EP2515853A2 Combination therapy for COPD The invention concerns an aerosol formulation suitable for administering to COPD patients by means of a pressurized metered dose inhaler (pMDI), comprising glycopyrronium chloride in combination with formoterol. The formulation further comprises a HFA propellant, a co-solvent, and an amount of inorganic acid sufficient to stabilize both the glycopyrronium chloride and the formoterol components. Optionally the formulation further comprises beclometasone dipropionate.
CN101003541A Antibacterial compound in broad spectrum and usage This invention relates to an antibacterial compound, more specifically, 6-fluoro-1-methyl-4-oxo-7-(1-piperazine)-4H-[1, 3] thiazine [3, 2-a] quinoline-3-carboxylic glyconate (compound I), its preparation method and its application. Compound I is prepared by reaction of 6-fluoro-1-methyl-4-oxo-7-(1-piperazine)-4H-[1,3]thiazine[3,2-a]quinoline-3-carboxylic acid and gluconic acid. Compound I can be used as effective component and mixed with normal pharmaceutical carrier to manufacture antibacterial drug composition, which can be tablets, capsules, granules, injection, eye preparations, ear preparations, gynecological preparations, and external use preparations. Compound I has stable properties, and can be easily dissolved in water, thus can be easily manufactured into various preparations used in clinical treatment. The method has such advantages as simple and reasonable process.
US20120252862 Dissolvable Film Strip Comprising Natural Components The present invention relates to film strips which comprise natural product formulations and can be absorbed from oral mucosa. The said film strip can be used with the aim of preventing and treating diseases in a short time, by being absorbed rapidly when it is applied from the oral mucosa at lower dosages than the dosage forms known.
WO2004058770A8 Triptolide derivatives and their use Triptolide derivatives of Formula (I), their pharmaceutically receptable salts and optical isomers, Formula (I), (wherein, C5 and C6 connect with each other by a C-C single bond or double bond; when C5 and C6 are connected with C-C single bond, X and Y represents independently hydrogen, oxygen, hydroxy, halogen, lower alkyloxy, lower alkylamino, mercapto, lower alkylthio, the group of formula -OCOR, -OSO2OR or -OPO(OH)2, each of which is attached to C5 and C6, R represents -(CH2)nCO2Na, -(CO2)nCO2K, or -(CH2)nCH3, wherein n = 1-6; Z represents hydrogen, oxygen, hydroxy, halogen, lower alkyloxy, lower alkylamino, mercapto, lower alkylthio, the group of formula -OCOR, -OSO2OR or -OPO(OH)2, each of which is linked at C14-position, R represents -(CH2)nCO2Na, -(CO2)nCO2K, or -(CH2)nCH3, wherein n = 1-6; wherein, the “__” linked with X, Y, and Z represents “(a) ” or “(b)” , provided that X and Y cannot both be hydrogen atom at the same time), the methods for preparing them and their use as antiphlogistic agent, immunosuppressive agent or therapeutic agent for other related diseases.
US20110053939 Novel aromatic nitro compounds Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning—X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
CN103040725A Method for modifying dissolution of drospirenone by using grinding and drospirenone solid dispersion The invention belongs to the scientific field of pharmaceutic preparations, and in particular relates to a method for modifying dissolution of drospirenone by using grinding and drospirenone solid dispersion. The method comprises the following steps: (1) the drospirenone and hydrophilic non-polymer accessories or water soluble accessories are evenly mixed by the mass ratio of 1:(1-1):30; and (2) the evenly mixed materials are fully grinded or milled, and are screened. The method has the advantages of simple operation, low cost, simplicity, practicability and convenience in promotion; the preparation produced by drospirenone dispersion which is prepared by the method is quickly dissolved out; 80 percent of drospirenone can be furthest dissolved out in 10 minutes; and 98 percent of drospirenone can be furthest dissolved out in 20 minutes; the drospirenone is quickly dissolved out; the biological utilization rate is high; no organic solvent is remained; the stability is high; and the method is suitable for preparing solid preparation.
CN101264081B Compound for treating pulmonary fibrosis The invention discloses the usage of the compound in a structural formula I in preparing drugs preventing and / or treating lung fibrosis of mammalian. The drugs can be made into orally-taken administration formulation selected from tablet, capsule, powder, granule, crystal, solution, suspension, decoction, syrup, elixirs, tea and masticatory spasm and also can be made into inhale administration or insufflation administration, intranasal administration and transdermal administration or administration formulation selected from spray of nasal cavity, nasal drop, suspension, gel, ointment, cream, emulsion and powder.
CN103505424A Preparation method for bortezomib for injection The invention relates to a preparation method for bortezomib for injection. The preparation method comprises the following steps: (1) polylactic acid and tertiary butanol are weighed, and a certain quantity of injection water is added for dissolving to obtain a polylactic acid and tertiary butanol mixed solution; (2) bortezomib raw materials are weighed, added in the mixed solution, and stirred until the raw materials are dissolved totally; (3) mannitol is weighed, added in the solution with the dissolved raw materials, and the injection water is added to account for 70% of the total amount, then is quickly stirred until the mixture is completely dissolved; (4) 5 g of activated carbon is added and stirred for 20 minutes, then is filtered out; (5) the injection water is added to reach 9.5 L; the pH value is regulated to 4.0-7.0 by using sodium hydroxide or hydrochloric acid; then the injection water is added until the total amount achieves 10 L; (6) the vacuum freeze drying technique is adopted for freeze-drying after filling; the freeze-drying technique is as follows: the pre-freezing temperature is kept for -40 DEG C for 3 hours; the sublimation drying time is 16 hours; the resolve drying time is 4 hours; the total time is 23 hours.
WO2005095438A1 Saponins, the preparation and the use of the same The present invention relates to steroidal saponins, the preparation thereof, and the use of the same in prevention of cardio-vascular diseases of myocardial infarction or the like. The chemical formula of such steroidal saponins is the following general formula (I) or (II). In the invention, such steroidal saponins of formula (I) or (II) can be isolated from traditional Chinese medicines and natural products by several methods of isolation, or be obtained by synthesis and semi-synthesis. The oral or non-oral formulations can be formulated by conventional methods using single compound or the mixture of such compounds in the different proportion. Such formulations can be used for prevention of many cardio-vascular diseases of myocardial infarction, coronary heart disease, angina pectoris, arrhythmia, myocardial ischemia, hypertension, hyperlipidemia and blood viscous or the like. In the general formula (I) or (II), R1=ß-D-glucose; R2 linear sugar chain or branched sugar chain; R3=H or CH3.
WO2012149478A2 Agents useful for treating friedreich's ataxia and other neurodegenerative diseases This invention provides methods of identifying agents useful to prevent, ameliorate or treat one or more symptoms of Friedreich's ataxia or other neurodegenerative disease, and methods of employing the identified agents to prevent, reduce, delay or inhibit one or more symptoms of Friedreich's ataxia or other neurodegenerative disease.
CN101015541A Diacetyl rhein dropping pills and its preparing process This invention relates to a dripping pill of diacetyl rhein. the pill is characterised in that it is prepared from diacetyl rhein and dripping pill substrate at a weight ratio of 1:1-5. the preparation method comprises pulverizing diacetyl rhein, adding substrate, heating, stirring to fusion, moving to a dripping pill engine with the temperature of materials and dripper at 75-85deg.C, stirring, dripping into coolant at 0-6deg.C and speed of 40+-10 pill/min, separating the dripping pill and coolant through a separating unit, and dripping to obtain the final product. The invention has the advantages of few air contact, uneasy oxidation, no hydrolysis, increase medicine stability, and improved shelf life.
CN103212082A Novel load method of camptothecin anti-cancer drug The invention relates a novel load method of a camptothecin anti-cancer drug. A segmented copolymer of poly(N-3-aminopropyl methyl acrylamide hydrochloride)-b-poly(N-isopropyl acrylamide) can be synthesized by utilizing a reversible addition-fragmentation chain transferring polymerization method, a camptothecin organic solution is uniformly mixed with the segmented copolymer, a polymer micelle with the camptothecin is synthesized under the stimulation of the temperature, and then the glutaraldehyde or glutaric acid small molecular crosslinking agent is used for conducting the shell crosslinking reaction for the polymer micelle. A camptothecin drug carrier prepared by utilizing the method has excellent drug carrying performance, so that the camptothecin can be rapidly and high efficiently adsorbed under a certain concentration condition, but also the camptothecin can be timely, high efficiently and targetedly released in a specific environment. The method has the advantages of easy operation, high yield, low cost, no environmental pollution, wide application prospect and the like. The prepared camptothecin anticancer drug is a new generation high-performance drug carrier product and also can be used for conveying other anti-cancer drugs which are difficult to dissolve in the human body. The method is particularly applicable to the medical field for researching the tumor cells.
WO2012075393A2 Activators of proteasomal degradation and uses thereof The present invention provides compounds that induce gate opening of the proteasome, thereby activating the proteasomal degradation of proteins. Such compounds may have beneficial therapeutic effects. Compounds and compositions described herein may be used to treat disorders associated with unfolded, misfolded, or aggregated proteins such as sickle cell anemia, thalassemia, Alzheimer's disease, Parkinson's disease, cystic fibrosis, Huntington's disease, amyotrophic lateral sclerosis (i.e., Lou Gehrig's disease), and Creutzfeld-Jakob disease. The compounds and compositions may also be used to kill or inhibit the growth of a microorganism. The present invention also provides methods for identifying compounds that activate the proteasomal degradation of proteins. In particular, the present invention provides in silico methods for identifying compounds that activate the proteasomal degradation of proteins.
CN102860996A Method for preparing lycoypene microcapsule The invention discloses a method for preparing a lycoypene microcapsule. The method includes that lycoypene is prepared to be core materials and the core materials and wall materials are subjected to homogeneous emulsifying and spray drying. The wall materials are prepared by gelatins, sporoderm-broken ganoderma lucidum spore powders, cane sugars and skim milk powders, the weight ratio of the gelatins, the sporoderm-broken ganoderma lucidum spore powders, the cane sugars and the skim milk powders is 1:1:1:(1.2-1.6), and the core materials are prepared by the lycopene, salad oil and sucrose esters. According to the method for preparing the lycoypene microcapsule, a specific microcapsule technology is utilized to embed the lycoypene, the stability of the lycoypene microcapsule is improved, simultaneously the water solubility is improved, and the application field is widened.
EP1224187B1 Certain alkylene diamine-substituted heterocycles The present invention also provides a general method to whereby mono-, bi-, or tri-cyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula (I-XV).
EP2033638A2 Beta-lapachone for the treatment of pancreatic cancer A composition comprising β-lapachone, or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier, for use in the treatment or prevention of a cell proliferative disorder of the pancreas. Said cell proliferative disorder may be pancreatic cancer.
EP1829535A2 Tissue factor antagonists and methods of use thereof The invention includes tissue factor (TF) blocking compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such compounds. Compounds of the invention are particularly useful for treating or phrophylaxis of undesired thrombosis.
EP1742916A1 Phenyl compounds and their use in the treatment of conditions mediated by the action of pge2 at the ep1 receptor Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, Z, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine, in particular their use in the treatment of conditions mediated by the action of PGE2 at the EP1 receptor. The EP1 receptor is associated with smooth muscle contraction, pain (in particular inflammatory, neuropathic and visceral), inflammation, allergic activities, renal regulation and gastric or enteric mucus secretion.
CN101953799A Lamivudine powder and preparation method thereof The invention discloses lamivudine oral powder. The powder is prepared by sealing 20-300mg of lamivudine without any auxiliary materials with a proper pharmaceutical packaging material, such as a paper aluminum composite film or a strip composite packaging film (SP film for short), wherein the moisture content of lamivudine is controlled to be 0.1 to 0.5 percent, and the grain size is 80-100 meshes. The lamivudine powder is fast in vitro dissolution rate, strong in stability and reasonable in clinical application, saves the auxiliary materials and the process cost, has simple productive process, is relatively easier to meet the medicament standard, and is more suitable for large-scale industrialized production. Therefore, the invention provides a new kind of preparation for the clinical use of the lamivudine medicament.
CN103421001A Berberine hydrochloride crystal E form substance, preparation method, pharmaceutical compositions and applications The invention discloses a novel crystal E form substance of Berberine hydrochloride compound (chemical name: 5,6-dihydro-9,10 dimethoxy phenyl [g]-1,3-benzodioxole [5,6-a] quinolizine ydrochloride, English name: Berberine hydrochloride), a preparation method, pharmaceutical compositions and applications, concretely discloses a novel crystal E form solid substance state of Berberine hydrochloride compound, a preparation method for novel crystal E form solid substance samples, and applications of Berberine hydrochloride crystal form substance as an active component in preparation of medicines preventing nervous system diseases, cardiovascular system diseases, digestive system diseases, immune system diseases, inflammation and infectious diseases. The molecular structural formula of Berberine hydrochloride is shown in the specification.
CN1997360B Stable pharmaceutical composition of fluoroether compound for anesthetic use, method for stabilizing a fluoroether compound, use of stabilizer agent for precluding the degradation of a fluoroether com The present invention has as objective the stabilization of a fluoroether compound against degradation by acid substances. The stabilizers proposed are selected among appropriate pharmaceutical compounds selected from the group constituted of propylene glycol, polyethylene glycol, hexylene glycol and 1,3-butileneglicol, or a saturated cyclic alcohol preferably menthol, and are used for preparing stable pharmaceutical compositions of a fluoroether compound. Method for stabilizing a fluoroether compound and use of stabilizers agents for precluding the degradation of a fluoroether are also described.
CN101209238A Biological degradation type long-acting hypodermal contraception implant containing gestodene and preparation thereof The invention relates to the technical field of contraceptive drugs, in particular to a biodegradation type long-acting subdermal contraceptive implant containing gestodene which uses the biodegradable polymer materials as the carrier for preparation and the preparation. The invention consists of the drug gestodene and the polymer biodegradable materials which are taken as a carrier (such as, trimethylene carbonate/p-Dioxanone copolymer (P(TMC-co-PDO))), a bar-shaped drug core is prepared by mixing the drug and the carrier, then the carrier materials are prepared into a drug delivery tube, then the drug core is arranged in the drug delivery tube, and the both ends are blocked by adhesives. The average daily drug delivery amount of the drug gestodene in the body is 10 to 30 micrograms. The implantation of one implant can be contraceptive for 1 to 2 years. The carrier materials can be degraded into small molecules after the release of the drug, the invention does not need to be taken out by the operation method, and the using cost is greatly reduced.
US20100016315 Iminopyridine Derivative and Use Thereof Provided are an iminopyridine derivative having a selective α1D adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like, and a screening method for a compound having an α1D adrenergic receptor antagonistic action. An α1D adrenergic receptor antagonist containing a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof, and a method of screening for an agent having an α1D adrenergic receptor antagonistic action for the prophylaxis or treatment of a lower urinary tract disease, which includes measuring the bladder smooth muscle tension of rats with bladder outlet obstruction.
CN101856409A Medicinal composition for treating skin itch, preparation method and application thereof The invention provides a medicinal composition for treating skin itch, which is a preparation prepared from the raw material medicaments of cortex moutan radicis, densefruit pittany root-bark, lightyellow sophora root, liquorice root, borneol and menthol crystal. The invention also provides an external medicament which is prepared by taking paeonol extract used as active ingredients in the cortex moutan radicis, dictamnine extract used as active ingredients in the densefruit pittany root-bark, matrine extract used as active ingredients in the lightyellow sophora root, glycyrrhetinic acid extract used as active ingredients in the liquorice root, the borneol and the menthol crystal as active ingredients and adding pharmaceutically-acceptable auxiliary materials or auxiliary components. The invention also provides a preparation method of the medicinal composition. The medicament of the invention can treat the symptom of pruritus caused by accumulating evils of wind heat, moist heat and blood heat in the skin, comprising the pruritus caused by eczema. The medicinal composition of the invention has a refining formula of raw materials, definite material basis, definite curative effect and little toxic or side effect, and particularly has the unique curative effect on pruritus symptom of which the course of disease is lingering and repeated.
EP1791813B1 Pentafluorosulfanylphenyl-substituted benzoylguanidines, method for the production thereof, their use as a medicament or diagnostic agent, and a medicament containing these compounds The invention relates to pentafluorosulfanylphenyl-substituted benzoylguanidines, to a method for the production thereof, to their use as a medicament or diagnostic agent, and to a medicament containing these compounds. These pentafluorosulfanylphenyl-substituted benzoylguanidines are of formula (I), in which R1 to R5 have the meanings as cited in the claims, and are, for example, suited for use as antiarrhythmic medicaments with a cardioprotective constituent for preventing infarcts, treating infarcts and for treating angina pectoris. These compounds inhibit, even preventively, the pathophysiological processes in the occurrence of ischemically induced damages, particularly during the initiation of ischemically induced cardiac arrhythmias.
WO2012103119A1 Compositions for administering rifalazil and other anti-tuberculosis agents in unit dosage form for oral administration Pharmaceutical compositions including rifalazil, a surfactant, a lipophilic antioxidant, and one or more antibiotics selected from the group consisting of isoniazid, streptomycin, pyrazinamide, and ethambutol are provided in a single unit dosage form for oral administration. The compositions can be used to treat tuberculosis. By placing the multiple antibiotic agents in a single unit dosage form, patient compliance with otherwise complicated treatment regimens can be increased.
CN101698649B Short-acting hypnotizing and calming compound used for anesthetization The invention discloses a phenyl acetic vinegar compound shown in the general formula (I), wherein A represents CnHmFxClyBrz and at least has an alkyl group, a naphthenic group, an olefine group or an alkyne group which is substituted by a halogen atom; n in the A is 1-6, m is 0-2n, x is 0-2n, y is 0-2n, z is 0-2n, m+x+y+z=2n+1, 2n-1 or 2n-3, and x+y+z >= 1; and R1, R2 and R3 represent alkyl groups of C1-C6, olefine groups of C2-C6 or alkyne of C2-C6 which are respectively independent. The invention also relates to a medicine composition taking the compound as an active component and the application of the compound and the medicinal composition in an anesthetization maintaining, inducement and hypnotizing calmative of people or animals.
EP1909785A2 Use of progesterone receptor modulators The use of compounds of formula (I), or a pharmaceutically acceptable salt thereof, (I) wherein R1, R2, R3, R4, R5, R6 and R7, are as defined herein, for contraception, hormone replacement therapy, synchronizing estrus, treating dysmenorrhea, treating dysfunctional uterine bleeding, treating uterine myometrial fibroids, treating endometriosis, treating benign prostatic hypertrophy, treating carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, pituitary, and meningioma, inducing amenorrhea, cycle-related symptoms, or treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder are described. Also provided are products containing these compounds.
US20090176719 Compositions and methods for treating perioral dermatitis Methods for treating perioral dermatitis are described herein. The method includes administering topically a composition containing an effective amount of a systemic or topical antibiotic and a corticosteroid. The concentration of the antibiotic is from about 0.01% to about 5% by weight of the composition and the concentration of the corticosteroid is from about 0.01% to about 5% by weight of the composition. The composition can contain one or more pharmaceutically acceptable excipients and/or carriers. The compositions can be formulated as a lotion, cream, gel, ointment, paste, powder, solution, suspension, spray, foam, or patch.
US20080153758 6-[Amino(4-chlorophenyl)-1-methyl-1H-imidazol-5-ylmethyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone; (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2R)-2-Amino-3-mercaptopropyl]amino]-3-methylpentyl]oxy]-1-oxo-3-phenylpropyl]amino]-4-(methylsulfonyl)-butanoic acid 1-methylethyl ester; exhibit potent activity agains The invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention more specifically relates to new uses of compounds that inhibit the prenylation of proteins, in particular the geranylgeranyl and/or farnesyl modifications of proteins, for treating neurodegeneration involving oxidative stress and, more particularly, Parkinson's disease. The invention also relates to corresponding methods of treatment, and can be used in human subjects for preventive or curative treatment, either alone is or in combination with other active agents or treatments.
CN101283973A Sustained-release injection containing netilcosin A sustained-release injection containing netilmicin comprises sustained-release microspheres and solvent. The microspheres contain sustained-release adjuvants and aminoglycoside antibiotics, and the solvent is a special solvent containing suspending agent such as sodium carboxymethylcellulose and having viscosity of 100-3000cp (20-30 DEG C); and the sustained-release adjuvants are selected from poly(ethylene-co-vinylacetate) (EVAc), polifeprosan, poly(lactic acid) (PLA), poly(lactic-co-glycolic acid) (PLGA), sebacic acid copolymer, albumin glue and gelatin; the sustained-release microspheres can also be made into sustained-release implant or ointment. The sustained-release implant or injection can be locally placed or injected into foci to locally sustained-release of drug for 5-30 days, so as to obtain and maintain local drug effective concentration while remarkably reduce the systemic toxicity of the drug. The sustained-release injection has distinct and unique therapeutic effect on local infection diseases caused by Staphylococci, Streptococci, Peptostreptococcus, Propionibacterium acnes, Enterobacter, Mycobacterium tuberculosis, Gonococcus or Meningococcus, such as chronic osteomyelitis, severe decubital ulcer, refractory skin ulcer, diabetic foot, femoral head necrosis, abscess, etc.
WO2006106438A3 Modulators of ppar activity Disclosed are the methods for modulating the activity of a peroxisome-proliferator activate receptor (PPAR) in an individual comprising administering to said individual a therapeutically effective amount of a compound characterized by the presence of a hydrocarbon chain of variable length, e.g., 10-32 carbons, that is terminated at one end by a -COOH group or a salt or a functional derivative thereof. The compounds may be represented by formulae (I) and (II), where R1, R2, R3, R4, R5, R6 and X are disclosed in the specification.
EP2329816A1 An anti-cancer active substance from antrodia camphorata, method for preparing the same and use thereof An anti-cancer active substance from Antrodia Cinnamomea, produced from mycelium of Antrodia Cinnamomea with following steps: (1) culturing mycelium of Antrodia Cinnamomea by liquid fermentation ; (2) extracting the thus-obtained mycelium with ethanol and concentrating the extracted solution to obtain an ethanol extract ; (3) dissolving said ethanol extract in water, and extracting with equal volume of ethyl acetate to obtain ethyl acetate extrct ; (4) purifying said ethyl acetate extract by silica gel column chromatography using hexane/ethyl acetate gradient as the mobile phase to obtain an eluate fraction g ; and (5) purifying said eluate fraction g by silica gel column chromatography using hexane/ethyl acetate gradient as the mobile phase to obtain a specific eluate fraction which could be purified further to obtain said anti-cancer active substance from Antrodia Cinnamomea.
WO2009017455A1 A new combination of (a) an alpha-4-beta-2 -neuronal nicotinic agonist and (b) a gsk3 inhibitor The present invention related to a combination of (a) a α4β2-neuronal nicotinic agonist and (b) a GSK3 inhibitor. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treating CNS disorders in mammals by administrating said combination. The invention further relates to a kit comprising the combination and use of said kits in treatment of CNS disorders such as dementia and/or Alzheimer's Disease.
EP1565179B1 Composition comprising a carbamic acid derivative, its use as cosmetic and medicine The invention concerns a composition containing at least a carbamic acid derivative, optionally associated with at least one compound such as a metalloprotease inhibitor, a PKC inhibitor, an anti-inflammatory agent, a soothing agent, an immunosuppressor, an ion chelator, an oxazoline, and an alkanolamide. The invention also concerns such a composition for its use as medicine, in particular for its use for preventing or treating skin pathologies of allergic, and/or inflammatory and/or irritant origin or resulting from a danger signal. The invention further concerns a method for cosmetic treatment of skins and/or mucous membranes which are sensitive, irritated, intolerant, exhibit allergic tendency, aged, exhibit skin barrier disorder, or exhibit non-pathological immunologic imbalance, which consists in applying on the skin and/or mucous membranes such a composition.
CN102319249A Anti-leukemia small molecular compound targeting mir-150 The invention relates to a novel antitumor small molecular lead compound which is synthesized based on a drug virtual screening platform combining bioinformatics with computer technology, and has targeted inhibition effect on mir-150 synthesis. The small molecular compound has the advantages of good permeability, less toxic or side effect, simple structure, and easy synthesis. The compound can be combined with tumor necrosis factor (TNF-alpha) to enhance the tumor-killing effect of the latter, and thus has the effect of tumor treatment; therefore, the compound is expected to be developed into a novel antitumor drug.
CN1806802A Pharmaceutical composition with acetaminopher, loratadine and pseudoephedrine sulfate as active ingredients, preparation method and uses thereof The invention relates to a medicinal composition, method of preparation and use, wherein paracetamol, loratadine and pseudoephedrine sulfate are used as the medicinal active constituent, as well as pharmaceutically acceptable auxiliary materials. The composition can be used for treating seasonal allergic rhinitis and common colds, and can be prepared into tablets, capsules, effervescent tablets, chewable tablets, slow release capsules, and slow release capsules.
EP1507530B1 Diaminothiazoles and use thereof as cdk4 inhibitors The present invention is directed to novel diaminothiazoles of formula (I): These compounds inhibit cyclin-dependent kinase 4 (Cdk4) and are selective against Cdk2 and Cdkl. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to their use for the preparation of medicaments for the treatment and control of cancer, most particularly the treatment or control of breast, lung and colon and prostate tumors.
US7388010 fused hexacyclic derivatives consist of pyrrolidine, indazolone, quuinoxalinone rings; cyclin-dependent kinase inhibitor with cell growth-inhibitory activity; anticarcinogenic and antiproliferative agent A quinoxalinone derivative of the formula (I): or a pharmaceutically acceptable salt or ester thereof, wherein; X is NH, S or the like; Y is O or the like; the partial structure is, for example, the formula: B1, B2, . . . , Bn−1 and Bn, (in which n is 4, 5 or 6) are each independently CH, N or the like; B′1, B′2, . . . , B′n−1 and B′n (in which n is 4, 5 or 6) are each independently hydrogen or the like; and R is hydrogen, lower alkyl or the like.
CN1629309A Method for screening acceptor blocker for controlling prawn virus infection Disclosed is a method for screening acceptor blocker for controlling prawn virus infection, wherein the combined analytic technique for virus and prawn cell membrane protein is employed for the screening process of the virus receptor bonding blocking agent, and screening is achieved by comparing the influence of the screening article treatment to the combination of virus and prawn cell membrane protein, the three screened substances have blocking-up action to the combination of leukoplakia syndrome virus and prawn branchia cell membrane.
CN103479604A Derivatives of n-(arylamino) sulfonamides including polymorphs as inhibitors of MEK as well as compositions, methods of use and methods for preparing the same This invention concerns N-(2-arylamino) aryl sulfonamide compounds which are inhibitors of MEK including crystalline polymorphic forms which exhibit a specific powder x-ray diffraction profile and/or a specific differential scanning calorimetry profile. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein. The invention also concerns methods of making the compunds and compositions described herein.
CN102068458A Eyesight improving product The invention discloses an eyesight improving product. The product is prepared from the following raw materials in weight percent by a conventional method: 1-20% of ocustilla, 1-20% of B-carotene and 60-98% of raw materials of chewing gum; the product can be also prepared from the following raw materials in weight percent by the conventional method: 1-40% of the ocustilla, 1-40% of the B-carotene and 20-98% of the raw materials of the chewing gum; and taste additives can be also added based on the same weight percent. The eyesight improving preparation disclosed by the invention has the advantage that the ocustilla is added to the chewing gum, thus facilitating eyesight treatment for a user when the user chews the gum.
WO2012052745A1 Combinations of pi3k inhibitors with a second anti -tumor agent There is provided combinations comprising (A) a compound of formula (I), wherein R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, together with (B) one or more therapeutics agents/treatments known to be useful in the treatment of diseases such as cancer or a proliferative disease, which combinations are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
CN1875946A Nanoparticle of 10-hydroxycamtothecine and preparation method thereof The invention discloses 10-hydroxycamptothecin solid nano particles and its preparing process, which comprises 10-hydroxycamptothecin, carrying agent, stabilizing agent and water, wherein the carrying agent is selected to be new auxiliary materials of POGC, PEG or PEGC, the obtained particles have the advantages of high medicament carrying quantity and good stability.
CN102824374A Preparation method of polysaccharide anti-oxidative tablets The invention relates to polysaccharide anti-oxidative tablets which are a novel product currently invented. The product is prepared from plant polysaccharide and sodium selenite. The product contains an agaric amino acid which is rare in plants, tricholoma acid, and wheat sterol. The substances have functions of anti-oxidation and free-radical resisting. The substances can be used for controlling various diseases. The tablets provided by the invention can be used for preventing the occurrences of various diseases.
EP1622607A1 Angiotensin ii receptor blockers for preventing the development or progression of microvascular disease due to diabetes The invention relates to the field of inhibitors of angiotensin II receptor blockers and particularly addresses their use in diabetes to prevent the development or progression of microvascular disease (i.e. disease involving small blood vessels) affecting eyes (diabetic retinopathy) and kidneys (diabetic nephropathy).
CN1980931A Compounds with atypical antipsychotic activity. Formula (I) compounds with atypical antipsychotic activity where the meanings of the various groups are as described here below, are endowed with activity characteristic of atypical antipsychotic agents, and therefore are useful as medicaments, particularly for the treatment of schizophrenia, paranoid states, manic-depressive states, affective disorders, social regression, personality regression and hallucinations.
US6982351 Cycloalkyl substituted polyamines for cancer therapy and methods of synthesis therefor Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
WO2012160713A1 Learning and memory improver The present invention aims to provide antidementia agents which are free from the problem of side effects and are excellent in safety. The present invention also aims to provide agents for improving learning and memory which are useful for improvement of learning and memory and can be ingested continuously. The present invention provides antidementia agents and agents for improving learning and memory, each comprising a cyclic dipeptide with the 2,5-diketopiperazine structure as an active ingredient.
CN1895297A Medicine for treating beriberi and its preparation A medicine for treating beriberi is proportionally prepared from golden larch bark powder, benzoic acid, salicylic acid, miconazole nitrate, clobetasol propionate, medical vaseline and medical alcohol. Its preparing process is also disclosed.
CN101991692A Composited medicine for treating hircismus The invention relates to a composited medicine for treating hircismus, which is characterized by being prepared from 50 granules of black pepper, 50 granules of wild pepper and 2 pieces of borneol by proportion through the steps of: crushing, pulverizing, uniformly stirring, homogenizing with 70-75% alcohol (in a proper amount), bottling and sealing. The composited medicine has good curative effect and low medicine prices, can be applicable to vast crowds, and is particularly suitable for poor people having low household income and living in remote villages far away from towns.
US7858656 Controlled release formulations containing an active ingredient, preferably melatonin and the method of preparation A controlled release melatonin tablet having a slow release nucleus of melatonin, hydroxypropyl methylcellulose, a lubricant, a volume excipient and a glidant, wherein 95% of the melatonin is released within 5 hours in an oscillating tray containing gastric/intestinal juice at 37° C. and a fast release cortex coating on said nucleus of melatonin, hydroxypropyl methylcellulose and a volume excipient, wherein at least 95% of the melatonin is released within 10 minutes in an oscillating tray containing gastric/intestinal juice at 37° C.
US20130022609 Method of treating androgen independent prostate cancer The present invention is directed to a method treating prostate cancer. The method comprises administering to a patient in need thereof at least one compound selected from N-methyl-Δ3,3′-dihydroindole-2,2′ diketone; N-1-(β-D-O-triacetyl-xylopranosyl)-Δ3,3′-dihydroindole-2,2′ diketone; and N-1-(β-D-O-triacetyl-xylopranosyl)-N′-methyl-Δ3,3′-dihydroindole-2,2′ diketone. Preferably the compound is in an amount sufficient to inhibit growth, invasion, and/or metastasis of prostate cancer cells.
US20050080022 substituted benzylphenol derivatives as intermediates for glucopyranosyloxybenzylbenzene derivatives; agents for the prevention or treatment of diabetes, diabetic complications, obesity or the like The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a hydroxy(lower alkyl) group; and R2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a hydroxy(lower alkyl) group, a hydroxy(lower alkoxy) group, a hydroxy(lower alkylthio) group etc., and salts thereof, which have an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, obesity etc., and intermediates thereof.
US6924388 Bicyclic aromatic compounds and pharmaceutical/cosmetic compositions comprised thereof Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds having the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): and Ar2, X1, R1, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined in the specification.
US20080306142 Isolation, purification and synthesis of procyanidin B2 and uses thereof Methods for the synthesis, isolation, and purification of procyanidin B2 are disclosed. The synthetic methods utilize epicatechin as a starting material and produce procyanidin B2 in high yields. The isolation methods extract procyanidin B2 from a sample of bark powder from plant matter of the genus Uncaria. The isolated and/or synthesized procyanidin B2 is used to treat amyloid disease, such as Alzheimer's disease and Parkinson's disease as well as improve cognitive performance and increase learning and memory in Alzheimer's patients. Pharmaceutical compositions containing the synthesized and/or isolated procyanidin B2 are also disclosed.
US20100144845 Oligonucleotide systems for targeted intracellular delivery The present invention provides methods for deriving oligonucleotides for specific internal delivery to one or more target cell types (e.g., cancer cells). The method generally includes selecting at least once with a target cell type to provide a plurality of internalizing oligonucleotides for the target cell type, and in some embodiments, counter-selecting at least once with a non-target cell type to provide a plurality of oligonucleotides that do not bind to features present in the non-target cell type. Therapeutic and diagnostic compositions including the oligonucleotides, and methods of treatment are also provided.
US20090022816 Storable, consumable pre-nascent iodine This discovery is storable, pre-nascent iodine that activates and: produces nascent iodine over a two-to-three-hour period within the body when diluted in water and consumed. The iodine is in a low concentration in a tincture of grain alcohol. A quantity of tincture is submerged in a glass container in an electrolytic bath between two electrodes and subjected to a specific amperage for a period of time. This action causes the diatomic bond of the iodine molecule to be broken with the iodine atom receiving excitation energy from the magnetic field. When diluted and consumed into the body, the nascent iodine is able to produce significant beneficial effects in the body.2
CN1561982A Bumetanide dripping pill and its preparing method A dripping pill of bumetanide is prepared from superfine pulverizing and conventional steps for preparing dripping pills.
CN103417949A TCM composition for treatment of male sterility The invention relates to TCM composition for the treatment of male sterility. The composition is made with, by weight, Psammosilene Tunicoides root, chingma abutilon seed, Lapis Chloriti, rhizome of broadleaf common Valeriana, dried longan pulp, fruits of Polygonum Orientale, fewflower lysionotus herb, Turpinia leaf, sea-ear shell, leaf of purpleflower holly, tabasheer, common lophatherum herb, stiff silkworm, dried ginger, toad venom, Chinese Torreya seed, small centipeda herb, Zaocys dhumnades, indigoplant leaf, manyinflorescenced sweetvetch root, stalactite, pummelo peel, Szechwan chinaberry fruit, common dayflower herb, pine nodular branch, Chinese honeylocust spine, alpine yarrow herb, ophicslcite, scorpion, humifuse euphorbia herb, dried black soybean sprout, cockscomb flower, Philippine violet herb, lotus leaf, wild buckwheat rhizome, rhizome of paniculate Bolbostemma, root of whiteflower hogfennel, common coltsfoot flower, Chinese starjasmine stem, Japanese ampelopsis root, Chinese wax gourd peel, common Jasminorange leaf and twig, gorgon euryale seed, Chinese ligusticum rhizome, leaf of paniculate microcos, long pepper, longtube ground ivy herb, Divaricate Saposhnikovia root, fruit of Rangoon creeper, and Chinese honey locust. The TCM composition is all made of natural materials, is high in safety, has specific curative effect, and is applicable to large-scale clinical popularization.
CN102925291A Variable pressure distillation method for extracting pythoncidere and essential oil from Chamaecyparis plants The invention relates to a variable pressure distillation method for extracting pythoncidere and essential oil from Chamaecyparis plants. The pythoncidere is aqueous solution, and contains main effective ingredients including borneol, cedrol, carvacrol, bisabolol, and the like. The essential oil from Chamaecyparis plants is yellow and contains cedrene, thujopsene, cedrol, and the like. The variable pressure distillation process comprises the following steps: drying and pulverizing rhizomes of Chamaecyparis obtusa and Chamaecyparis formosensis, filling into a distillation tank, introducing steam from lower steam inlet of the distillation tank for 30-50 s, starting an oil pump to vacuumize so as to generate negative pressure of 40-60 kpa, reducing pressure and humidifying after pressure stabilizes, gradually restoring the negative pressure to normal atmospheric pressure after 20-30 min, connecting a coiled condenser for condensing vapor after 20-30 min, decolorizing with about 50-100 g activated carbon, separating oil phase and water phase, and filtering to remove impurities with filter screen to obtain the essential oil and hydrosol from Chamaecyparis plants, namely, water-soluble pythoncidere.
US20090062362 Veterinary Formulation for Administration of a Water-Insoluble Drug to a Target Animal Through a Water Distribution System This invention concerns a method for the preparation of a suspoemulsion formulation, which can be easily produced on an industrial scale and which allows the reproducible and effective administration of one or more water-insoluble veterinary drugs through water distribution systems. The water-insoluble veterinary drug, in finely ground form, is dispersed in a water immiscible liquid, followed by homogenisation of this system into a water phase. To facilitate the preparation of a stable formulation, one or more stabilising agents such as emulsifiers, thickeners, anti-oxidants and anti-microbials can be used. The resulting suspoemulsion shows excellent long term storage stability and a good “in use” stability after dilution in a vessel and during all handling and transport in the water distribution system.
EP1077715B1 Use of rosmarinic acid and derivatives thereof as an immunosuppressant or an inhibitor of sh2-mediated process The present invention relates to use of rosmarinic acid and/or derivatives thereof as immunosuppressive agents and/or as inhibitor of SH2 domain function. Disclosed in the present invention is that rosmarinic acid and derivatives thereof specifically inhibit the binding of ligand peptides to Lck SH2 domain, disturb the Lck-mediated signal transduction in T cells, also inhibit cytokine gene expression, and suppress immune responses in the transplanted tissue. These activities of rosmarinic acid and derivatives thereof support their applicability to treatment, prevention and/or diagnosis of graft rejection, GVHD, autoimmune diseases, inflammatory diseases, etc.
US20110313031 Olioodeoxynucleotide and its use to induce an immune response A substantially pure or isolated oligodeoxynucleotide of at least 10 nucleotides is disclosed, wherein the oligodeoxynucleotide comprised a sequence represented by either formula: 5′N1N2N3T-CpG-WN4N5N63′ wherein the CpG motif is unmethylated, W is A or T, and N1, N2, N3, N4, N5, and N6 are nucleotides, or the formula: 5′RY—CpG-RY3′ wherein the central CpG motif is unmethylated, R is A or G, and Y is C or T, as well as an oligodeoxynucleotide delivery complex and a pharmacological composition comprising the present inventive oligodeoxynucleotide, and a method of inducing an immune response by administering the present inventive oligodeoxynucleotide to a host. In some embodiments, the oligodeoxynucleotide includes the nucleic acid sequences set forth as SEQ ID NO: 137.
US7759385 opioid receptor ligands such as {4-[3-(1H-indol-3-yl)-pyrrolidine-1-yl]-1-phenyl-cyclohexyl}-dimethylamine dihydrochloride salt, used as analgesics The invention relates to 4-substituted 1-aminocyclohexane corresponding to formula (I) to a method for the production thereof, to pharmaceutical formulations containing these compounds and to the utilization of 4-substituted 1-aminocyclohexane compounds for the production of pharmaceutical formulations and related methods of treatment.
US20110098797 Drug eluting composite The present invention relates to materials having therapeutic compositions releasably contained within the materials. The materials are configured to release therapeutic compositions at a desired rate. The present invention also relates to devices incorporating the materials.
CN102219748A Amorphous Ambrisentan and preparation method thereof The invention provides amorphous (+)-(2S)-2-[(4,6-diemthyl pyrimidine-2-yl)oxy]3-methyoxy-3,3-diphenylpropanoic acid (Ambrisentan). The graph of the Ambrisentan is detected by virtue of X-ray powder diffraction. The invention further provides a preparation method of the amorphous Ambrisentan. The preparation method comprises the following steps: dissolving crystalline Ambrisentan solid into one solvent or a mixture of multiple solvents so as to prepare a solution, or directly preparing an Ambrisentan reaction solution; and carrying out spray drying on the solution, spraying into water and then stirring so that the amorphous Ambrisentan is separated out, or directly pouring the solution into water so as to collect the amorphous Ambrisentan. The amorphous Ambrisentan in the invention is easier to be prepared into medicament preparations. Compared with the Ambrisentan serving as a water-indissoluble medicament for preparing the preparations, the amorphous Ambrisentan in the invention has a good dissolution release behavior. And simultaneously, the preparation method of the amorphous Ambrisentan is easy to industrialize and has strong production adaptability.
CN103214427A Crystal form and application of R-pramipexole The invention belongs to the field of medicinal chemistry and particularly relates to a crystal form of R-pramipexole hydrochloride. An X diffraction angle 2theta (+/-0.2) of powder of the R-pramipexole hydrochloride is about 6.408 DEG, 7.190 DEG, 14.399 DEG, 18.471 DEG, 23.463 DEG, 24.190 DEG, 26.856 DEG, 29.075 DEG and 36.495 DEG. The preparation method comprises the following steps of: adding free alkali of the R-pramipexole into a certain quantity of organic solvent, introducing hydrogen chloride, stirring the mixture at the temperature of 0-50 DEG C for 0-24h, carrying out suction filtration to obtain a crude product, and crystallizing the obtained crude product in a C1-C4 alcohol solvent to obtain the crystal form.
WO2009089399A3 Compositions comprising toll-like receptor or coreceptor antagonists and methods for ocular neuroprotection Compositions for treating or controlling degeneration of at least a component of the human optic nerve system comprise an antagonist to a toll-like receptor, a coreceptor thereof, or a combination thereof. The compositions can also include an anti- inflammatory medicament. Such compositions can be administered to provide neuroprotection to a patient suffering from an ocular disease, such as glaucoma, AMD, DR, or retinitis pigmentosa.
WO2007110214A1 12-aza-ep0thil0nes, process for their preparation and their use as antiproliferative agents The invention relates to 12-aza-epothilones of formula (I), wherein R1 is optionally substituted aminocarbonyl, optionally substituted alkoxycarbonyl, aryloxycarbonyl or heteroaryl and R2 is a radical of formula (II), wherein X is S, O, NR4, -C(R5)=N-, -N=C(R5)- or -C(R5)=C(R6)-; and R3, R4, R5 and R6 are as defined in the specification, and which is bound to the radical of formula (I) at one of the two carbon atoms indicated with an asterix; a method of manufacture of these compounds, new intermediates, pharmaceutical preparations containing these compounds, and the use of these compounds in the treatment of proliferative diseases. These 12-aza-epothilones are highly potent cytotoxic compounds and are active against multidrug-resistant cell lines and tumours.
US20060264393 Methods for evaluating genetic susceptibility and therapy for chronic inflammatory diseases The invention discloses a knockout mouse that is homozygous for a RUNX3 null allele, as a novel model for chronic inflammatory disease. The present invention provides methods for treating T cell-related inflammatory conditions by cell therapy, gene therapy or antisense for up regulating or down regulating RUNX3. The invention further relates to methods of diagnosing and assessing predisposition to chronic inflammatory diseases. The present invention further provides methods for testing agents for effectiveness in treating and/or preventing diseases associated with chronic inflammatory or autoimmune conditions.
US7005430 Such as (R)-2-cyclopentyl-7,8-dihydro-8-(4-picolyl)-4-(n-propyl)-1H-imidazo(2,1 -i)purin-5(4H)-one d-tartaric acid, which has glucose concentration-dependent insulin secretion promoting action/hypoglycemic activity; antidiabetic agents A condensed purine derivative represented by Formula (I): wherein X—Y-Z represents R1N—C═O or N═C—W, R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, V1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, V2 represents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when V1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X—Y-Z represents R1aN—C═O and R2 represents a substituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted alicyclic heterocyclic group, a halogen atom, a lower alkylthio group, —NR7R8, —CO2H, a lower alkoxycarbonyl group, —COHal, —CONR9R10 or —CHO, V2 may represent a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group; or a pharmacologically acceptable salt thereof.
WO2008067177A2 Methods for the treatment of alcohol abuse, addiction and dependency The present invention is directed to methods for the treatment of alcohol abuse, addiction and / or dependency, alone and in combination with one or more anti-addiction agents.
CN101574318B Preparation method of taxol injection The invention provides a preparation method of taxol injection, comprising the following steps: (1) blending polyoxyethylene castor oil and molecular sieve, and filtering and degerming; (2) removing trace moisture in taxol, and filtering and degerming; (3) blending, filtering and degerming solutions obtained in step (1) and step (2),. The method avoids overlarge local concentration or low whole content caused by overlong time used for blending solutions or incomplete solution of materials, thus solving the uniformity problem of solution of materials and the stability problem of the taxol injection in the process of blending solutions.
US20120088773 Circadian rhythm modulation A method and composition is herein described to modulate the circadian rhythm to effect summer metabolism and the metabolic syndrome. The method entails the once daily, timed ingestion of a dopamine precursor or a dopamine agonist, receptor primed with caffeine, and vitamin D3.
CN101884616A Docetaxel long-circulating liposome and preparation method thereof The invention aims to provide a method for preparing a docetaxel long-circulating liposome. The method comprises the following steps of: dissolving docetaxel and carrier materials such as phospholipid, cholesterol and the like together in an organic solvent; forming a film through rotary evaporation in a 40 to 70 DEG C water bath; adding buffer solution which contains a surfactant and performing refrigeration at the temperature of below 4 DEG C for 10 to 60 minutes to fully hydrate the film; and then mixing or stirring to obtain the docetaxel liposome. The liposome of 70 to 500nm is prepared from the docetaxel and can be prepared into docetaxel long-circulating liposome frozen powder for injection by lyophilization.
EP1453916B1 Combination containing a poloxamer and chondroitin sulphuric acid and/or a glycoprotein and use thereof The invention concerns a novel combination for use in a hydrating cosmetic formulation of a poloxamer and a polymer selected among a glycoprotein or chondroitin sulphuric acid. The invention also concerns its use in a cosmetic formulation, the cosmetic composition containing said combination and the corresponding cosmetic treatment. The novel combination can also be used for preparing ocular compositions for treating dry eye syndrome, but also for preparing buccogingival and vaginal solutions for treating dryness.
WO2010132992A1 Compounds for the inhibition of herpesviruses 3D protein modeling and virtual screening of commercially-available compounds were performed to identify new inhibitors of the herpesvirus DNA polymerase, a key enzyme in the viral replication cycle. Two compounds (Nos 2 and 9) were particularly active against HSV-1 and HSV-2 strains and one compound (No 3) inhibited specifically cytomegalovirus (CMV) strains (overall hit rate of 25%). Some of the tested compounds inhibited wild-type viruses and strains resistant to current antiviral agents. New chemical entity derivatives of compound 2 with binding potential to the DNA polymerase retained an excellent activity against HSV-1, HSV-2 and VZV like the parental compound, as well as against strains resistant to current antiviral agents. These non-nucleosidic herpesvirus DNA polymerase inhibitors with in vitro activity against drug-resistant clinical isolates warrant further pre-clinical studies.
EP1131290B1 Piperidine ccr-3 receptor antagonists This invention relates to certain piperidine quaternary salts of formula (I), that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
EP1633871A1 Double-stranded nucleic acid The invention is directed towards constructs for RNAi techniques. The invention provides a ribonucleic acid (RNA) for use as interfering RNA in gene silencing techniques to silence a target gene comprising in a 5' to 3' direction at least a first effector sequence, a second effector sequence, a sequence substantially complementary to the second effector sequence and a sequence substantially complementary to the first effector sequence, wherein the complementary sequences are capable of forming double stranded regions with their respective effector sequences and wherein at least one of these sequences is substantially identical to the predicted transcript of a region of the target gene, and a nucleic acid construct encoding such an RNA.
EP2694051A1 Use of l-carnitine, salts and derivatives thereof for reducing or preventing fatigue and improving cognitive function The invention relates to the use of L-carnitine, a salt of L-carnitine, a derivative of L- carnitine and/or salt of a derivative of L-carnitine, as well as respective methods and 5 compositions, for reducing or preventing fatigue and/or for improving cognitive function in an animal. The animal is preferably a healthy individual and the use is preferably a non-therapeutic use.
CN101269040A Pioglitazone hydrochloride sustained-release dropping pill and preparation method thereof The invention discloses to a drug compound for treating diabetes and particularly relates to a drug compound oral pharmaceutical formulation adopting pioglitazone as the ingredient. The drug compound aims to supplement the deficiency of the prior oral pharmaceutical formulation used for treating Type-2 Diabetes and provide a drug compound oral pharmaceutical formulation, sustained-release pioglitazone dropping pill which has high bioavailability, controllable release time, long-acting effect, low frequency of drug taking, steady plasma concentration, low cost and absence of contamination during the production. The sustained-release pioglitazone dropping pill adopts pioglitazone as the chemical ingredient and is prepared jointly with the medicinal carriers of hydrophilic frame ingredients and hydrophobic frame ingredients used as the stroma.
CN101744945A Oral liquid for adjusting gastrointestinal function The invention discloses an oral liquid for adjusting the gastrointestinal function, which belongs to a health care medicine and aims at providing an oral liquid for promoting the appetite and the digestion and improving the immunocompetence and the gastrointestinal function. The oral liquid is prepared from 10-100g of hawthorn, 8-50g of Chinese date, 1-10g of medlar, 1-10g of roxburgh rose, 1-10g of calcium lactate, 10-100g of zinc lactate, 1-10g of taurine and 1-10g of stachyose. The oral liquid is prepared by using the following method: mixing the hawthorn, the Chinese date, the medlar and the roxburgh rose, adding water and decocting for two times; preparing liquid extract with the relative density of 1.15-1.25 (70DEG C); mixing the calcium lactate, the zinc lactate, the taurine and the stachyose, adding water and dissolving, evenly mixing with the liquid extract, adding water to 1,000ml and evenly stirring; and extracting filtrate. The invention has the advantages of convenient taking, good for mouthfeel, suitability for both children and adults and the like and is a heath-care medicament improving the gastrointestinal environment and the immunocompetence.
WO2010011845A3 Preventing or treating viral infection using an inhibitor of the lsd1 protein, a mao inhibitor or an inhibitor of lsdl and a mao inhibitor An embodiment of the invention provides preventing or treating a viral infection of a host, comprising administering to the host an effective amount of an inhibitor of the protein LSD1 and/or a monoamine oxidase inhibitor. Another embodiment of the invention provides preventing or treating reactivation of a virus after latency in a host, comprising administering to the host an effective amount of an inhibitor of the protein LSD1 and/or a monoamine oxidase inhibitor. Another embodiment of the invention provides preventing or treating a viral infection in a mammal that has undergone, is undergoing, or will undergo an organ or tissue transplant, comprising administering to the mammal an effective amount of an inhibitor of the protein LSD1 and/or a monoamine oxidase inhibitor before, during, and/or after the organ or tissue transplant. The viral infection may be due to a herpesvirus, such as herpes simplex virus type 1 (HSV-1) or type 2 (HSV-2), varicella zoster virus (VZV), or cytomegalovirus (CMV). The viral infection may also be due to an adenovirus, including types 1-5.
US20110218206 Individual and combination of mdivi-1 and nutlin-3 for topical or intravitreal ophthalmic use Disclosed are pharmaceutical compositions comprising mdivi-1 and nutlin-3, individually and in combination, for topical or intravitreal ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma, optic neuropathies including Leber Hereditary Optic Neuropathy, arteritic or non-arteritic Ischemic Optic Neuropathy, and retinal artery and vein occlusions.
CN101516893A Novel 5, 7-disubstituted [1, 3 ] thiazolo [4, 5-d] pyrimidin-2 (3h)-one derevatives and their use in therapy The invention discloses novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.
US7648983 Inhibits beta -secretase or beta -site amyloid precursor protein-cleaving enzyme (BACE); Alzheimer's disease; S)-4-(2,4-difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine The present invention provides BACE inhibitors of Formula I: methods for their use, and intermediates and methods for their preparation.
WO2006091795A3 METHODS AND COMPOSITIONS INVOLVING EXPRESSION OF α1C SUBUNIT OF L-TYPE CALCIUM CHANNELS IN SMOOTH MUSCLE CELLS The present invention concerns methods and composition for modulating the level of gene expression of the α1C subunit of the L-type calcium channel. Such methods and compositions provide preventative and therapeutic benefits with respect to gastrointestinal motility disorders. In examples of the invention, sustained changes in gene expression of the α1C subunit are effected by a low dose of a modulator given over an extended period of time. This provides methods and compositions for inducing sustained contractility or relaxation of gut smooth muscle cells.
US20110129536 Nanocomposite materials based on metallic nanoparticles stabilized with branched polysaccharides The present invention provides nanocomposite systems made of metallic nanoparticles stabilized with branched cationic polysaccharides, in particular alditolic or aldonic mono- and oligo-saccharidic derivatives of chitosan, and their preparation obtainable with aqueous solutions of these polysaccharides in the presence or absence of reducing agents. The peculiar chemical and physical-chemical features of these polysaccharides allow to form metallic nanoparticles homogeneously dispersed in the polysaccharidic matrix and an effective stabilization thereof. The properties associated with the nanometric dimensions and the presence of biological signals on polymeric chains may be exploited in applications with antimicrobial activities and of molecular biosensors.
US20120283261 Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase In one aspect, the invention relates to substituted N-phenylpyrimidin-2-amine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of Axl kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the Axl kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
CA2323810C Ophthalmic solution comprising glycogen An ophthalmic solution comprising a sterile aqueous solution of a glycogen polysaccharide.
US20100056545 Novel phenylacetate derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and composition for prevention or treatment of diseases induced by activation of t-type calcium ion channel containing the same as an active ingredient Disclosed herein are a new phenylacetate derivative represented by Chemical Formula 1 or pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for prevention or treatment of diseases induced by the activation of T-type calcium ion channels containing the same. The composition containing the phenylacetate derivative according to the present invention effectively inhibits the activation of T-type calcium ion channels and may be useful in the prevention or treatment of diseases such as hypertension, cancer, epilepsy, and neurogenic pains induced by the activation of T-type calcium ion channels. wherein, X, R1, and R3 are as defined herein.
US20110190386 Aptamer Inhibitors of Osteopontin and Methods of Use Thereof The present invention polynucleotide aptamers that selectively bind to and inhibit the function of osteopontin, pharmaceutical compositions comprising the same, and methods of use for diagnostics and treatment of diseases and disorders associated with osteopontin.
US20100239659 Self-assembling amphiphilic polymers as anti-cancer agents The invention provides amphiphilic biocompatible copolymers which have a hydrophilic backbone and pendant hydrophobic groups. The polymers form nanoscale molecular aggregates in aqueous environments, which have hydrophobic interiors within which anticancer drugs may be solubilized. The polymers optionally feature attached antibodies, receptor ligands, and other targeting moieties which mediate adherence of the drug-carrying aggregates to targeted cancer cells.
EP2762134A1 Composition for treatment of pathogens that are resistant to tetracyclines The invention relates to compounds and pharmaceutical compositions useful in combination with tetracyclines in the treatment of bacterial infections caused by Gram-positive and Gram-negative pathogens, with particular efficacy in tetracycline resistant strains. These compounds specifically bind to TetR and therefore prevent the transcriptional activation of tet resistance genes. The compounds have a potentiating effect on the activity of members of the tetracycline family, in particular of tetracycline, minocycline, doxycycline and tigecycline, in the treatment of tetracycline susceptible, intermediate and tetracycline resistant pathogens.
US7378413 2-amino-3-(alkyl)-pyrimidone derivatives A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted. And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β such as Alzheimer's disease.
CN103239636A Application of reed rhizome extract and gingerol in preparation of attenuated synergistic medicines for cancer chemotherapy The invention relates to a natural pharmaceutical composition, a preparation method of the natural pharmaceutical composition, and an application of the natural pharmaceutical composition in preparation of attenuated synergistic medicines for cancer chemotherapy. The natural pharmaceutical composition is prepared from reed rhizome extract and gingerol according to the ratio of (3-24):1. The composition has an excellent curative effect on side effects such as vomiting and the like caused by cancer chemotherapy, and can play a role in inhibiting tumors.
US20080153775 Weight reduction program and method A new weight reduction program and method 1 having three phases, an acute weight loss phase 2, a transitional phase 3 and a long-term maintenance phase 4. Appetite suppressants 12 (such as phenylkylamine sympathomimetic amine 13), calcium pyruvate 17, a multiple vitamin-mineral supplement 16, amino acids and cyanocobalomine 10 are taken in conjunction with the new diet program to achieve optimal weight loss and health benefits.
WO2008092199A1 Thiopyrimidine-based compounds and uses thereof The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.
EP2303924A2 Lm-antibodies, functional fragments, lm-1 target antigen, and methods for making and using same The invention provides LM-1 antibodies, functional fragments, modified and variant forms, nucleic acid and other compositions. The invention also provides antibodies, functional fragments, modified and variant forms that bind to LM-1 antigen (e.g., NONO/nmt55). Antibodies, functional fragments, modified and variant forms, nucleic acid and other compositions are useful in treatment and diagnostic methods. One method includes treating metastasis of a neoplasia, tumor or cancer in a subject in need of treatment by administering to the subject an amount of a LM-1 antibody, an antibody that binds to LM-1 antigen, or a functional fragment thereof, effective to treat metastasis of the neoplasia, tumor or cancer in the subject.
WO2014100353A1 8'-hydroxy-dihydroergotamine compounds and compositions 8'-HydiOxy-Dihydroergotamine (8'-OH DHE) medicinal compounds, compositions, and dosage forms containing such compositions are provided. Also provided herein are methods of treatment, prevention, or amelioration of diseases, conditions or disorders selected from amyotrophic lateral sclerosis (ALS), Parkinson's disease, stress/anxiety, nausea, emesis, aggression, pain, neuropathic pain, sleeplessness, insomnia, restless leg syndrome and depression using the compounds, compositions, dosage forms and administration techniques disclosed herein.
CN102670549A Ropinirole hydrochloride osmotic pump type controlled release tablet The invention provides a ropinirole hydrochloride osmotic pump type controlled release tablet, which adopts ethyl cellulose and polyvinylpyrrolidone as semipermeable membrane formation materials, an asymmetric tablet type is preferable, the ageing phenomenon of the semipermeable membrane can be overcome, and the medicine residue is lowered. The invention also provides a method for improving the anti-ageing performance of the ropinirole hydrochloride osmotic pump type controlled release tablet. The method is characterized in that the ethyl cellulose-polyvinylpyrrolidone is adopted to serve as the semipermeable membrane material. In addition, the invention also provides an application of the ethyl cellulose-polyvinylpyrrolidone composite to prepare the ropinirole hydrochloride osmotic pump type controlled release tablet with the anti-ageing performance.
US7098375 Animal and cell models for type II diabetes and their use A transgenic diabetes type II model laboratory animal is disclosed which comprises β-cells expressing a dominant negative form (dnFGFR1c) of FGFR1c. Also disclosed is the use of the Ipf1/pdx1 promoter for controlling expression of FGFR1c; β-cells in which the expression of PC1/3 is down-regulated or absent or which are competent to express a dominant negative form (dnFGFR1c) of FGFR1c; mature β-cells incompetent to express Glut2 or in which the processing of proinsulin is substantially impaired; a method of preventing or treating type II diabetes.
EP2294063B1 Pyrrolidine ether derivatives as nk3 receptor antagonists The present invention relates to a compounds of formula I wherein R1, R2, R3, R', Ar, o, n and m are as defined in the specification. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
WO2010031589A1 Small molecule bradykinin b2 receptor modulators The present invention is related to a compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein R1 is: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m), (n), (o), (p), (q), (r), (s); R2 is C1, F, or methoxy; R3 is methyl, methoxy, hydroxymethyl, H, or absent; R4 is methyl, ethyl, HO, H, or absent; A1 is C or N; A2 is C or N; R6 is H or OH; R5 is: (t), (u), (v), (w), (x), (y), (z).
US20100120910 Cosmetic Compositions Comprising Esters Based on 2-Propylheptanol The invention relates to the use of esters of 2-propylheptanol with benzoic acid and/or benzoic acid derivatives in cosmetic and/or pharmaceutical preparations. The compounds are distinguished by their particularly light sensory impression.
WO2005014611A1 The artificial cpg single strand deoxidation oligonucleotide and its antiviral uses The present invention disclosed a set of artificial ODNs which contain one or more CpG(s), the said ODNs can stimulate human PBMC to produce antiviral substances. These antiviral substances make cell avoid of the attack from virus, the influenza virus and the single strand plus RNA virus are preferred, such as hepatitis C virus, dengue virus and Japanese encephalitis virus. Moreover, the antiviral uses of artificial CpG ODNs and its uses for treating and preventing viral infection are also provided.
US20090076080 Deuterium-enriched fexofenadine The present application describes deuterium-enriched fexofenadine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN101829060A Preparation method of clindamycin phosphate powder for injection The invention discloses a preparation method of clindamycin phosphate powder for injection, comprising the following steps of: taking clindamycin phosphate, adding alkaline solution at room temperature, stirring for dissolving the clindamycin phosphate to prepare sterile solution having a high concentration; in the sterile environment, adding inorganic acid or organic acid to adjust the pH value of the solution, adding inert organic solvent to crystallize, depressurizing, filtering and drying to obtain sterile powder of clindamycin phosphate; under the sterile condition, packing the powder in a sterile vial, covering the vial with a butyl latex plug, rolling a aluminum cover so as to make sterile powder. Compared with a prior art, the invention has the advantages of low cost, simple production device, short production cycle and the like; and dissolution of samples at a high temperature is unnecessary in the production process, which prevents the clindamycin phosphate from being dissolved or damaged in the production process, so that the final product has the advantages of high purity (low impurity), little toxicity and side effects and stable quality. The invention is particularly suitable for large-scale production.
WO2010117170A2 Pharmaceutical composition for treating or preventing burn injuries The present invention relates to a pharmaceutical composition for treating or preventing burn injuries, wherein said composition comprises, as active ingredients, compounds expressed in a specific chemical formula, or to pharmaceutically acceptable salts thereof or solvates thereof. Thus, the present invention provides a pharmaceutical composition for treating or preventing burn injuries, containing, as active ingredients, the above-mentioned compounds, or pharmaceutically acceptable salts thereof or solvates thereof, and also provides a method for treating burn injuries comprising the step of administering the above-mentioned compounds or pharmaceutically acceptable salts thereof or solvates thereof to the entity requiring treatment of a burn injury.
US7691859 prenyl transferase inhibitors; e.g. 8-butyl-7-(3-(imidazol-5-yl)-1-oxopropyl)-2-(2-methoxyphenyl)-5,6,7,8-tetrahydroimidazo[1,2a]pyrazine; antitumor agents; cancer of breast, colon, pancreas, prostate, lung, ovarian, epidermal; hematopoietics; Ras-dependent tumor; A family of imidazole compounds useful for inhibiting the activity of prenyl transferases. The compounds are covered by the following formula: wherein X is (CHR11)n3(CH2)n4Z(CH2)n5 where Z is O, N(R12), S, or a bond; Y is CO, CH2, CS, or a bond; R1 is or N(R24R25); and the remaining substituents are as defined in the disclosure.
CN1813748A Novel medicinal composition and its formulation The present invention discloses a medicine composition for curing hepatic disease and tumor radiotherapy and its preparation. Said medicine composition is made up by using ligustrazine and kurarinone according to the weight mixing ratio of 1:0.2-50 through a certain preparation process. Said medicine composition can be made into oral preparation and injection preparation.
CN101229188B External medicine for onychomycosis The invention provides an externally used medicine for onychomycosis treatment, relating to a medicine of treating onychomycosis. The invention solves the problems that seepage force to nail plates of the externally used medicine in the prior art, which cannot seep into the bottom or the deep level of the nail plate to kill fungi. The invention is prepared by mixing the following components by weight portions: povidone lodine of 24 to 36 portions, aspirin of 96 to 144 portions, polyethylene glycol of 44 to 68 portions, ethanol of 400, 480 to 720 portions and water of 91 to 137 portions. The externally used medicine for treating onychomycosis of the invention has the advantages of large seepage force and good treatment effects for onychomycosis, without recurrence after cure.
WO2006117029A1 Use of polylysine in combination with either green tea or olive extracts or both for use against halitosis The invention discloses ingredients and formulations with enhanced efficacy and long duration effect for use against halitosis (unwanted bad breath), resulting from the synergistic effect of the use in the formulation of a mixture of (epsilon)-polylysine with polyhydroxyphenolic compounds, such as green tea extracts (that contain polyphenolic compounds and/or epigallocatechingallate) or olive extracts (that contain oleuropein and/or hydroxytyrosol) or a combination of them. It discloses also a new production procedure for preventing the occurence of precipitation when mixing (epsilon) polylysine and green tea extracts. The ingredients and formulations can be used in mouth rinses, mouth sprays, gels, tablets that dissolve in the oral cavity, chewing gums, candies, artificial saliva.
WO2011058149A1 Tricyclic pyrazol amine derivatives This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.
CN101129326A Method of preparing smectite suspension agent The invention provides a montmorillonite mixing-floating agent for treating loose bowel movement and making method, which comprises the following steps: (1) drawing formulating amount montmorillonite, correcting agent, preservative agent, anddeionized water; (2) adding the montmorillonite into the anddeionized watert to stir uniformly to add the correcting agent and the preservative agent to stir uniformly; (3) producing the mixing liquid to form the uniform mixing-floating agent with grain fineness of the montmorillonite less than10mu m through colloidal mill that can be placed with homogenizer or ultrasonic machine; (4) sterilizing to split charging to get the mixing-floating agent. The invention has merits of fitting viscosity for splitting dose accurately and reducing production cost without assisting-floating agent, which makes the montmorillonite disperse thoroughly through the colloidal mill with finer grains that can be distributed in body's digestive tract rapidly after taking and with better effect.
CA2387762C Process of making substituted pyrazoles Disclosed is a process of making substituted pyrazoles (1) from substituted benzophenone hydrazones (11) with a variety of 13-bifunctional substrates (III) under acid conditions. The pyrazole compounds are useful for making pharmaceutical compounds. In said formula, wherein X is chosen from -CN and -C(O)-R3 wherein if X is CN then R3 in the product formula (I) is amino.
WO2012011112A1 Non psychoactive cannabinoids and uses thereof The present invention provides dihydro-CBD compounds of formula (I) and derivatives thereof, compositions comprising them and uses thereof in the manufacture of medicaments for the treatment of conditions, diseases, disorders or symptoms associated with inflammation.
US20120283268 Thiazole and Thiophene Analogues, and Their Use in Treating Autoimmune Diseases and Cancers Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.
WO2014138833A1 Compounds, use, pharmaceutical composition for inhibiting reductase in microorganisms, inha binder and method for obtaining inha binders The present invention describes new compounds for binding and/or inhibiting enzymes in microorganisms. In one embodiment, the compounds of the present invention are used to inhibit the 2-trans-enoyl-ACP (CoA) reductase enzyme in microorganisms, and are therefore useful as antimicrobial agents.
CN101954085A Method for preparing magnetic-targeted thermochemotherapy gold shell nano-drug delivery system The invention discloses a method for preparing a magnetic-targeted thermochemotherapy gold shell nano-drug delivery system, which comprises the following steps: preparing Fe3O4 magnetic nano-nucleus by using FeCl3 @6H2O and FeCl2 @ 4H2O as raw materials through a chemical precipitation process; and then plating a layer of gold shell on the surface of magnetic nanoparticles by using a self-assembly-electroless plating method, washing the prepared particles, and dissolving the prepared particles with pure water, then mixing the prepared particles with NIPAM and AA, and forming a temperature sensitive and controllable macromolecule polymer layer on the surface of the gold shell by using ammonium persulfate as initiator and under ultrasonic conditions. The diameter of a PNIPAM @ Au Fe3O4 particle prepared by using the method of the invention is 230 to 250nm, and the magnetic saturation strength thereof is 12.5 to 17emu/g, and the PNIPAM @ Au Fe3O4 particle shows super-paramagnetism. The particles prepared by using the method of the invention can load anti-neoplastic drugs into PNIPAM, and transfer near infrared radiation into thermal energy by using the gold shell layer, thereby realizing the function of releasing the drugs, and finally treating cancers through the principle of thermal ablation and chemotherapy.
CN103202889A Ointment for treating acne rosacea The invention discloses ointment for treating acne rosacea. The ointment comprises, by weight, 2-4 parts of sulfur, 2-4 parts of rhubarb and 6-20 parts of vaseline. The sulfur and the rhubarb are ground to obtain powder with the size of 150-300 meshes, the powder and vaseline are mixed and uniformly stirred to obtain paste, and the paste can be applied to treating the acne rosacea. The ointment has the advantages that the ointment can realize effects of performing disinfection, relieving itching, killing parasites, treating the acne rosacea, removing damp-heat and stasis and performing detoxification; as shown by clinical trials for the ointment, the treatment effective rate is 100%, and the recovery rate is higher than 98%; and as compared with existing anti-inflammatory bactericidal drugs, the ointment is particularly obvious in treatment effect, can be used safely and conveniently and is free of toxic or side effect.
WO2007125823A1 Composition comprising polysaccharide having immunomodulating function as main ingredient An object is to establish a process for production of a novel polysaccharide from a cassis polysaccharide (CAPS), wherein the novel polysaccharide can show a higher immunomodulating effect per unit amount, has a low viscosity, and can be handled readily during the process for producing a final product. Another object is to provide a health beverage/food having high safety and an excellent immunomodulating effect at a low cost by utilizing a juice, a processed juice or a purified product. Thus, disclosed is a composition mainly comprising a novel polysaccharide having an average molecular weight of about 10,000 to 40,000, wherein the polysaccharide is produced by a restrictive and partial enzymatic digestion of a CAPS. Also disclosed is an immunomodulating beverage/food using the composition.
WO2008144916A1 Method of reducing side effects of isoniazid This invention relates to a method of reducing the side effects of isoniazid. Specifically, the invention relates to administration of pyridoxal 5'-phosphate to reduce or mitigate the side effects of isoniazid. Also provided is the use of pyridoxal 5'-phosphate in the preparation of a medicament for the reduction of the side effects of isoniazid, a pharmaceutical composition comprising isoniazid and pyridoxal 5'-phosphate, and kits comprising pyridoxal 5'-phosphate and instructions for use of same to combat the side effects of isoniazid.
WO2006067114A1 Sulfonyl amino cyclic derivatives and use thereof The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
EP1900362A2 Alfa-aminoamide derivatives useful in the treatment of restless legs syndrome and addictive disorders Methods of using certain α-aminoamide derivatives in the treatment of RLS and addictive disorders. The compounds of this invention are able to reduce or even stop the symptoms of RLS and addictive disorders substantially without side effects.
CN103261196A Pyrazolopyridines as inhibitors of the kinase lrrk2 The present invention relates to compounds of formula I, or pharmaceutically acceptable salts or esters thereof, (Formula I) wherein R1 is selected from: aryl;heteroaryl; -NHR3;fused aryl-C4_7-heterocycloalkyl;-CONR4R5;-NHCOR6; -C3-7-cycloalkyl,-NR3R6; -OR3;OH; NR4R5; and alkyl optionally substituted with a substituent selected from R11 and a group A; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7- heterocycloalkyi are each optionally substituted with one or more substituents selected from C1-6-alkyl, C3-7-cycloalkyl, heteroaryl, C4-7-heterocycloalkyl, aryl and a group A, and said C1-6-alkyl, C3-7-cycloalkyl, heteroaryl, C4-7-heterocycloalkyl, and aryl substituents are in turn each optionally substituted with one or more groups selected from R11 and a group A; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, heterocycloalkyi, fused aryl-C4-7-rheterocycloalkyl and halogen, wherein said C1-6-alkyl,C2-6-alkenyl, aryl, heteroaryl,fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted with one or more substituents selected from R11 and A. Further aspects relate to pharmaceutical compositions and therapeutic uses of said compounds.
US20120045418 Pharmaceutical preparation comprising supernatant of blood mononuclear cell culture The present invention relates to a topical pharmaceutical preparation for treating an inflammatory skin condition, preferably a condition associated with ischemia, comprising a supernatant of a physiological solution obtainable by cultivating peripheral blood mononuclear cells (PBMCs) or a subset thereof in a physiological solution free of PBMC-proliferating and PBMC-activating substances for at least 1 h.
US20100130425 Use of toll-like receptor ligands in treating excitotoxic injury, ischemia and/or hypoxia Methods of protecting cells against cytotoxic insults are provided. The methods involve administering a composition including a Toll-like receptor (TLR) ligand, for instance a TLR7, TLR8, or TLR9 ligand to a subject. The methods are applicable to the protection of neural and non-neural cells. For example, methods of protecting a neural cell against excitotoxic brain injury are provided. Methods for preparing medicaments for the prophylactic treatment of excitotoxic injury, ischemia and/or hypoxia are also provided. Also provided are compositions for use in the described methods.
WO2014066851A1 C-myc antisense oligonucleotides and methods for using the same to treat cell-proliferative disorders Provided herein are antisense oligonucleotides that can effectively prevent or decrease c-myc protein expression as well as decrease overall rates of cell proliferation in in vitro and mammalian in vivo models of cell proliferative disorders as well as methods for using the same. The antisense oligonucleotides comprise at least one phosphoramidate (NP)-modified or thiophosphoramidate (NPS)-modified intersubunit linkage.
WO2011146819A3 METHODS AND COMPOSITIONS FOR TREATMENT NF-κB-MEDIATED AND α7 INTEGRIN-SUPPRESSED DISEASES The invention features compositions, methods, and kits useful for the treatment of diseases mediated by NF-κΒ and diseases suppressed by α7 integrin.
CN102138922A Cefcapene pivoxil hydrochloride composition and preparation method thereof The invention relates to a cefcapene pivoxil hydrochloride composition and a preparation method thereof. The composition consists of a tablet core and a coating layer, wherein the tablet core contains cefcapene pivoxil hydrochloride, a filler, a disintegrating agent and a lubricating agent; the grain diameter of the cefcapene pivoxil hydrochloride serving as a raw material is less than 100 micrometers; and the filler consists of a starch filler and soluble auxiliary materials, and the soluble auxiliary materials are in an amount which is 3 to 15 percent of the weight of the tablet core. The prepared cefcapene pivoxil hydrochloride tablets have excellent disintegrative property and dissolution of over 75 percent.
CN102188452A Formula of strong bone capsule The invention relates to a formula of a strong bone capsule. The invention discloses the formula of the strong bone capsule for preventing and improving osteoporosis through improving human microcirculation. The strong bone capsule comprises the following components: propole, calcium citrate, calcium gluconate, vitamin D and the like.
WO2007138334A2 Methods for identifying an agent that modulates type i or type ii pip kinase activity or expression Methods for modulating apoptosis and neurite outgrowth in cells by modulating levels of PtdIns(4,5)P2. Agents for such modulation, including agents which inhibit or activate type I and type II PIP kinases, and methods for identifying such agents. Methods for treating or preventing hyperproliferative disorders and neurodegenerative diseases using such agents.
WO2008086678A3 The medical use of levo-phencynonate as neuroprotective agent Levo-phencynonate and its nontoxic pharmaceutically acceptable salt having neuroprotective effect, the composition comprising these compounds as active components, and the use as neuroprotective agents. The structure of levo-phencynonate is represented by formula (Ia).
CN103127522A Conjugate of fatty acid-curcumin derivative and application thereof The invention provides a conjugate of a fatty acid-curcumin derivative and an application of the conjugate of the fatty acid-curcumin derivative. The structure of the conjugate of the fatty acid-curcumin derivative is shown as a formula (I). The curcumin fatty acid conjugate can largely improve the stability of curcumin, and the conjugate and a hydrophobic part of a carrier m PEG 2000-PLGA can easily form a compact hydrophobic core to form stable nanoparticle with particles around 100nm diameter, drug loading capacity is high, and the conjugate has a good liver target. The drug effect concentration of the curcumin in liver tissue can be greatly improved. The curcumin fatty acid conjugate nanoparticle can be suitable for tumours, especially for treatment of diseases of cancer of the liver.
EP0990654B1 Substituted cyclobutylamine derivatives Substituted cyclobutylamine derivatives with novel structures represented by general formula (I), wherein R1 to R4 and Q represent each a specific substituent and, in particular, Q represents a quinolone derivative of a specific structure. These derivatives are useful as antibacterial compounds which have excellent antibacterial actions over a wide scope of bacteria including gram-negative and gram-positive ones, exert potent antibacterial activities particularly on methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae and quinolone-resistant bacteria and are excellent in the in vivo dynamics and safety.
WO2014071128A1 Macrophage-derived matrix vesicles: an alternative mechanism for microcalcification in atherosclerotic plaques The invention relates to methods for decreasing, inhibiting, preventing, or reducing matrix vesicle induced calcification by inhibiting the amount or formation of a complex comprising phosphatidylserine (PS), annexin II, annexin V or VI, and S100A9 or S100A12 in a macrophage.
US7038077 2-Amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives; nervous system, psychological, and psychiatric disorders This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.
US20110039915 IMMUNOSTIMULATORY siRNA MOLECULES The present invention relates to a double-stranded siRNA molecule that is capable of silencing gene expression as well as inducing an immune response. The molecule comprises a sense strand and an antisense strand, wherein the antisense strand comprises a first nucleotide sequence that is specifically complementary to mRNA transcribed from a target gene, and the sense strand comprises a second nucleotide sequence that is substantially or perfectly complementary to the antisense strand with the exception that the second nucleotide sequence comprises at least one immunostimulatory motif comprising two or more non-complementary nucleotides. Such a molecule may be utilized in a method of treating or preventing a disease or condition (such as a viral infection, a bacterial infection, or cancer) in a subject.
EP1267867B1 Use of prostanoid ep4 receptor antagonists for the treatment of headache and assays for such antagonists The present invention provides for the treatment of primary headache disorders, particularly migraine, using antagonists of the EP4 receptor for prostaglandin E2. Particular EP4 receptor antagonists include azole compounds of formula (I) wherein R1 is a group such as a lower alkyl substituted with carboxy; R2 is hydrogen or lower alkyl, R?3 and R4¿ are aryl optionally substituted with halogen, Q is formula (II) in which -A1- is a single bond or lower alkylene, Formula (III) is a cyclo group, -A3- is a single bond or lower alkylene, and X is O, NH or S; or a salt or its solvate thereof.
CN1883483A An injection liquid for treating rheumatism The invention discloses a tuduranine hydrochloride injection for joint cavity injection and acupuncture point injection, wherein 1ml of the injection contains 12-40mg of tuduranine hydrochloride. The invention can realize less specification requirement, convenient operation,accurate dosage, and less adverse effect.
EP1550462B1 Remedy or preventive for kidney disease and method of diagnosing kidney disease It is intended to disclose a novel remedy or preventive for a kidney disease and a method of diagnosing (detecting) a kidney disease. The above-described remedy or preventive for a kidney disease contains a casein kinase 2 inhibitor as the active ingredient. The above-described method of diagnosing a kidney disease comprises measuring the activity or content of casein kinase 2 or the expression dose of a casein kinase 2 gene in a sample separated from a living body.
WO2012070043A1 Method and composition for weight-gain management Presented herein is a methodology for reducing weight in obese subjects and in patients receiving various medical treatments that are accompanied with weight gain. The methodology allows for management of weight gain, management of triglyceride levels and weight reduction in obese subjects.
WO2009139710A1 Quinuclidine derivatives and their use as muscarinic receptor antagonists The invention provides compounds of formula (I) wherein R1, R2, R3, Het1, n, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation
CN101518541A Application of liquiritin apioside The invention provides an application of liquiritin apioside for preparing medicine and health-care products for relieving cough, preventing asthma and eliminating phlegm. The liquiritin apioside is prepared singly or by matching with other active components or accessories. The liquiritin apioside has stronger medical effects for relieving cough, preventing asthma and eliminating phlegm, and can improve the symptoms of acute cough, chronic cough, profuse sputum and hyperpnea through the evaluation of main pharmacodynamics of liquiritin apioside preparation. The liquiritin apioside preparation can be made into any one preparation used in clinic, for example, capsule, tablet, oral liquid agent, and the like. The liquiritin apioside originates from natural plants, has rich raw material sources, low manufacture cost, little medicine toxic side effect, and obvious healing effect, and provides optimized natural medicine for clinically curing the symptoms of acute cough, chronic cough, profuse sputum and hyperpnea.
US20120149744 Anti-mitotic anti-proliferative compounds Substituted triazole compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a pathology linked to a hyperproliferative disorder by administering the substituted triazole compounds to a patient in need thereof.
US20080175810 Topical compositions for cosmetic and pharmaceutical use This invention relates to topical compositions in the form of dispersion gels formed by dispersing into an aqueous gel phase a substantially homogenous organic solution containing at least one active ingredient and at least one organic polymer solubilized in an organic carrier. The organic carrier comprises at least one water-miscible organic solvent and at least one water-immiscible organic solvent. The polymer is selected to affect efficacy of the compositions. The compositions are essentially free of surface-active substances and have favorable galenic properties.
CN103070934A Summer health-care foot washing liquor and preparation method thereof The invention relates to a summer health-care foot washing liquor which comprises the following components: 1 to 10 parts of belvedere fruit, 1 to 10 parts of mint, 1 to 6 parts of radix sophorae flavescentis, 1 to 10 parts of ageratum, 1 to 10 parts of milkwort, 1 to 6 parts of boric acid, 1 to 6 parts of salicylic acid, 1 to 6 parts of alkanolamide and 1 to 6 parts of cocoalkanoylamido propyl betaine. The preparation method of the summer health-care foot washing liquor comprises the following steps: 1, the belvedere fruit, the mint, the radix sophorae flavescentis, the ageratum and the milkwort in the formula are added in water, soaked and then decocted twice and are decocted for 1.5 hours each time; 2, the decocted liquid is filtered and then concentrated into clear paste; and 3, boric acid, salicylic acid, alkanolamide and cocoalkanoylamido propyl betaine are added in the clear paste. The summer health-care foot washing liquor has the effects of evacuating wind heat, relieving summer-heat, clearing damp, removing soil, sterilizing, protecting the skin, treating ringworm of the feet, and the like, and has the advantages of simplicity in production and convenience in use.
WO2007023154A2 Iron (iii) complex compounds for treating iron deficiency in patients with chronic inflammatory intestinal diseases The invention relates to the use of iron (III) complex compounds comprising carbohydrates or derivatives of the latter for producing a medicament for the oral treatment of conditions caused by an iron deficiency in patients with chronic inflammatory intestinal diseases, in particular Crohn's disease and ulcerative colitis.
US20100290989 Compositions affecting hyaluronic acid mediated activity Compositions comprising hyaluronic acid (HA) or agents that interfere with HA binding of HA receptors and methods of using the same are provided. For example, there is provided a composition comprising HA oligomers ranging in size from 10-mer to 80-mer and use of the same for promoting migration, growth or survival of wild-type or transformed/cancerous cells. There is also provided a composition comprising an agent that interferes with binding between an HA oligomer of a size of about 10-mer to about 80-mer and an HA receptor. Such compositions may be useful for therapeutic, diagnostic or imaging applications. Examples of therapeutic use are wound repair or cancer treatment.
CN101434560A Alkyloxycarbonyl substituted abricycline derivative The invention pertains to the technical field of medicines and particularly relates to a tetracycline derivative substituted by alcoxyl formoxyl shown in a general formula (1), pharmaceutically acceptable salts or isomers thereof; wherein, R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7> and R<8> are as defined in the instruction book; the invention also relates to preparation methods of the compounds, pharmaceutical composition containing the compounds and applications of the compounds in the preparation of medicaments for curing and/or preventing tetracycline-sensitive diseases.
US20080058292 Administering synergistic mixture of adipocyte proteinG antagonist and peroxisome proliferator activator antagonist; concurrent administering niacin and non-steroid antiinflammatory drug The present invention provides a method for reducing flushing in a patient and for for increasing HDL and/or HDL-2b levels in a patient, with compositions being administered to the patient only twice a day, from 30 to 60 minutes after lunch and 30 to 60 minutes after dinner. In some embodiments, the compositions include an adipocyte G-protein antagonist, a PPAR-α agonist, and a PPAR-γ agonist in amounts effective in to provide a synergistic therapeutic HDL increasing effect, and/or a synergistic therapeutic HDL-2b increasing effect.
US20100317668 Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
US20080069866 Immunotherapeutic methods and compositions This invention relates to methods and compositions introducing chemical entities into antigen presenting cells. The resulting presentation of said antigens on the surface of the antigen presenting cells gives an effect on the immune system. The invention also relates to the resulting modified antigen presenting cells and pharmaceutical compositions containing these cells. The invention discloses new understandings in adjuvancy and adjuvant preparations, including a series of related peptides and phospholipid vesicles incorporating said peptides.
WO2005032559A1 Nitric oxide donating derivatives for the treatment of cardiovascular disorders Compounds for inducing the expression of ApoA1, comprising a donatable nitric oxide moiety and a free-radical scavenging moiety. Preferably, nitric oxide derivatives of stilbenes, polyphenols, flavonoids and isoflavonoids and methods of their use are provided for treating patients suffering from diseases including hypercholesterolemia, vascular oxidative stress and endothelial dysfunction.
US7351714 viral infections; lung tumor and gastric cancer; 7-2-(2-aminophenyldithio)phenyliminomethylcamptothecin Camptothecin derivatives of camptothecin of formula (I) wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index. Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.
CN102863353A Substituted phenyl acetate compound and application thereof The invention belongs to the fields of medicine and chemistry, and provides a substituted phenyl acetate compound with the structure shown by formula (I), which has short-acting sedative-hypnotic effect so as to be used for preparing anesthetic and sedative. The experiments prove that the substituted phenyl acetate compound has the anesthetic activity stronger than that of propanidid, and has the action time and the recovery time which are shorter and more foreseeable than those of propofol, thus having the characteristics of being high in anesthetic effect and medicine effect, low in toxic and side effects and the like.
WO2008008537A3 Combi) compositions for the treatment of mucormycosis. comprising iron chelator and antifungal agent The invention provides a composition including at least one iron chelating compound and at least one antifungal agent. The composition can include the iron chelating compounds deferiprone or deferasirox. An antifungal agent included in the composition can include a polyene antifungal agent, an azole antifungal agent or an echinocandin antifungal agent. The invention also provides a method of treating or preventing a fungal condition. The method includes administering to an individual having, or susceptible to having, a fungal condition a therapeutically effective amount of at least one iron chelating compound for a sufficient time to reduce the severity of a fungal condition, wherein the iron chelating compound comprises a non-siderophore or non-xenosiderophore relative to the fungal condition. A method of treating or preventing a fungal condition provided by the invention also can include administering to an individual having, or susceptible of having, a fungal condition a therapeutically effective amount of at least one iron chelating compound and at least one antifungal agent. Provided further by the invention is a method including prophylactic administration of the at least one iron chelating compound or at least one iron chelating compound and at least one antifungal agent prior to onset of the fungal condition.
US20090318565 Novel Compositions for the Enhancement of the Anti-oxidant Potential of Hydrogenated Curcuminoids or Combinations Thereof Disclosed are novel compositions for the enhancement of the anti-oxidant potential of natural or metabolite hydrogenated (1E,6E)-1,7-Bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione derivatives. It was discovered that the antioxidant potential of hydrogenated curcuminoids was highly enhanced when a closely structurally related 1,7-Bis(4-hydroxyphenyl)-3,5-heptanedione, exhibiting unexpectedly pro-oxidant properties, was removed from the compositions.
WO2008029868A1 Ocular fibrous neovascularization inhibitor The invention relates to a chorioretinal neovascularization inhibitor suitable for treating or preventing chorioretinal neovascularization diseases, such as versican siRNA containing a core site sequence of versican, which is one of the chondroitin sulfate proteoglycans, or chondroitin-4-desulfatase which desulfating the sulfate group at the 4-position of chondroitin sulfate proteoglycan as an example of examining an effect of accumulation of chondroitin sulfate proteoglycan (CSPG). The invention also relates to a method of inhibiting chorioretinal neovascularization based on the inhibition of accumulation of chondroitin sulfate proteoglycan (CSPG) by administering versican siRNA, chondroitin-4-desulfatase or the like to a subject, and a method of treating or preventing chorioretinal neovascularization diseases such as diabetic retinopathy utilizing the same.
US20100298412 Disulfide Chemotherapeutic Agents and Methods of Use Thereof Compositions and methods for the treatment of cancer are provided.
WO2012156531A9 Lysine demethylase inhibitors such as cyclylcylopropamine derivatives for use in the treatment of inflammatory diseases or conditions The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.
WO2008157408A2 Use of prodrugs of gaba analogs, antispasticity agents, and prodrugs of gaba b receptor agonists for treating spasticity Methods of treating spasticity by administering a colonically absorbable prodrug of a GABA analog having antispastic activity that is not directly mediated by the GABAB receptor, optionally in combination with an antispasticity agent or a colonically absorbable prodrug of a GABAB receptor agonist are disclosed. In particular, methods of treating spasticity by administering a colonically absorbable prodrug of gabapentin or a colonically absorbable prodrug of pregabalin, in combination with a colonically absorbable prodrug of R-baclofen are disclosed.
WO2014028886A1 Nutlin-3a for treatment of proliferative vitreoretinopathy The invention provides compositions and methods for treatment of proliferative vitreoretinopathy.
CN103044308A Compound extracted from antrodia camphorata and purpose thereof The invention relates to a compound extracted from antrodia camphorata. The invention also relates to a compound or a method for curing or preventing hepatitis C virus (HCV) or human immunodeficiency virus (HIV).
US20120308617 Phospholipid-based inhalation system The present invention includes a method for delivering medications deeper into the lungs and to the medications' pulmonary targets, which include bronchioles and alveoli. A first particularly preferred embodiment of the invention describes the use of two steps for delivery of a medication. In a first step, an aerosolized therapeutic composition or medication is administered into a patient's respiratory tract, wherein the patient may be any animal or human subject. Following the first step, an aerosolized surfactant is administered into the patient's respiratory tract that facilitates delivery of the aerosolized medication of the first step to the medication's pulmonary target. Another embodiment of the present invention contemplates an apparatus for the delivery of an aerosolized surfactant used that facilitates delivery of previously inhaled aerosolized medication.
US20100137391 Histamine H3 Agonist for use as Therapeutic Agent for a Lipid/Glucose Metabolic Disorder Disclosed are: novel use of an agonist histamine receptor H3 (e.g., Imetit) for prevention of obesity or the reduction of food intake; a method for evaluation of a compound for use as a therapeutic agent targeted to histamine receptor HR protein; and a compound provided by the method.
WO2014062596A1 2'-methyl substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases The present invention relates to 2'-Methyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3, are as defined herein. The present invention also relates to compositions comprising at least one 2'-Methyl Substituted Nucleoside Derivative, and methods of using the 2'-Methyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
EP1263426B1 Preparations for the non-traumatic excision of a nail The invention relates to a preparation containing preferably a hydrophilic film-former, water and urea. Said preparation contains urea in a quantity of between 70 and 90 % by weight and the hydrophilic film-former in a quantity of between 10 and 30 % by weight, the respective quantities being measured in relation to the non-volatile constituents. The preparations are suitable for the non-traumatic excision of diseased toe and finger-nails, for example of fungus-infested areas of toe and finger-nails.
CN101411702A Nefopam hydrochloride naproxen sodium compound sustained-release preparation and preparation method thereof The invention provides a nefopam hydrochloride naproxen sodium compound sustained-release preparation and a preparation method thereof. The compound sustained-release preparation is prepared by mixing a nefopam hydrochloride sustained-release micro-pill and a naproxen sodium enteric sustained-release micro-pill according to a specific dosage proportion. The method is to combine the nefopam hydrochloride and the naproxen sodium which are two different medicines used for easing pains in different positions to prepare the compound sustained-release preparation which has synergistic action of the two medicines, greatly improved pain easing effect and reduced toxic and side effect. The compound sustained-release preparation can reduce medicine taking times for each day, improve the compliance of a patient, control the blood concentration of the medicine and stabilize the blood concentration, and has higher bioavailability.
WO2013155447A1 Tiki inhibitors Modulators of Wnt activity, e.g., Wnt inhibitors, that act on TIKI proteins and inhibit TIKI-mediated cleavage of Wnt proteins, as well as methods of identifying such modulators and methods of use thereof.
WO2009123881A1 Purine derivatives as a3 receptor- selective agonists Disclosed are (N)-methanocarba adenine nucleosides, e.g., of formula (I) as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.
EP2305675A1 Indazoles, Benzothiazoles, and Benzoisothiazoles, and preparation and uses thereof The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the alpha7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
US8361787 Method for expression of small RNA molecules within a cell The invention provides methods and compositions for the expression of small RNA molecules within a cell using a lentiviral vector. The methods can be used to express doubles stranded RNA complexes. Small interfering RNA (siRNA) can be expressed using the methods of the invention within a cell, which are capable of down regulating the expression of a target gene through RNA interference. A variety of cells can be treated according to the methods of the invention including embryos, embryogenic stem cells, allowing for the generation of transgenic animals or animals constituted partly by the transduced cells that have a specific gene or a group of genes down regulated.
WO2008103185A3 Substituted carboxamides as group i metabotropic receptor antagonists This application relates to a substituted carboxamide compound of formula I, or a pharmaceutically acceptable salt thereof, as defined herein, a pharmaceutical composition thereof, and its use in treating pain.
CN103479602A Application of hydroxylamine derivatives in neural degenerative disorder treatment The present invention relates to a class of small bio-molecules hydroxylamine derivatives with effects of balance of palmitoylation of important proteins in body, reduction of decomposition of functional proteins in body, and acceleration of decomposition or re-use of proteins, wherein particularly the butyl hydroxylamine (nt-BuHA) compound with characteristics of the best effect and the lowest side effect is the preferable compound, the functions of the compounds are providing deacetylation effects for palmitate modified proteins maintaining life function in brain cells, such that the palmitate fat chain removed-function proteins can be easily re-used by human body or enter protein degradation circulation pathways so as to reduce oxidative stress due to ester acylated function protein deposition and nerve cell dysfunction and apoptosis due to ER stress and the like. Results show that the small molecule compounds can be used for prevention and treatment of various diseases caused by neural degenerative diseases.
EP1453508B1 Tempamine compositions and use against cellular oxidative damage A therapeutic composition comprised of tempamine for treatment of conditions caused by oxidative stress or cellular oxidative damage is described. In one embodiment, the tempamine is administered in a vehicle suitable to extend its blood circulation lifetime. For example, tempamine is loaded into the liposomes that provide an extended blood circulation lifetime for effective therapy against inflammation or cell proliferation.
US7144893 4-aryl quinols and analogs thereof as therapeutic agents The present invention pertains to compounds of the formula (1) which are, inter alia, antiproliferative agents, anticancer agents, antimycobacterial agents, antituberculosis agents, and/or thioredoxin/thioredoxin reductase inhibitor: wherein: Q is ═O or ═N—S(═O)2—RQ;RQ is —II or optionally substituted C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; Ar is optionally substituted C5-20aryl; RO is an oxy substituent; the bond marked α is a single bond or a double bond; the bond marked β is a single bond or a double bond; R3 and R5 are each independently ring substituents; R2 and R6 are each independently ring substituents; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for example, in the treatment of proliferative conditions, (e.g., cancer), mycobacterial infections (e.g., tuberculosis), and/or conditions mediated by thioredoxin/thioredoxin reductase
CN103751145A Ornidazole capsule with improved uniformity The invention provides an ornidazole capsule with improved uniformity, and the capsule includes 20-30% of ornidazole, 20-45% of a filler, 6-12% of a disintegrating agent, an adhesive and a proper amount of lubricant. The filler is selected from the group consisting of lactose, sucrose, glucose, sorbitol, mannitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, starch, carboxymethyl starch, pregelatinized starch, microcrystalline cellulose and dextrin. The disintegrating agent is selected from the group consisting of cross-linked polyvinylpyrrolidone, pregelatinized starch, microcrystalline cellulose, alginic acid and sodium carboxymethyl starch. A preparation method of the ornidazole capsule with improved uniformity provided by the invention comprises the following steps: fully mixing ornidazole with the filler, disintegrating agent and adhesive, preparing the mixture into wet particles, drying by a fluidized bed, sieving through a screen of 18 mesh, adding 0.5% of magnesium stearate, tabletting, crushing, sieving through a screen of 14 mesh, and filling into capsules to obtain the ornidazole capsule.
US20060057229 External skin preparations for suppressing sebum secretion A drug for external application to the skin, for inhibiting sebum secretion, comprising a matrix metalloproteinase inhibitor.
CN101829118A Cefamandole nafate composition powder injection The invention provides a cefamandole nafate composition, which comprises the following components in percentage by mass: 99.00 to 99.99 percent of cefamandole nafate hydrate crystals and 0.01 to 1.00 percent of sodium benzoate. The cefamandole nafate composition powder injection prepared by the composition has the advantages of low hygroscopicity, high active medicament stability, no solvent residues and no degradation in long-term storage, and has the great superiority in medicinal preparations.
US7635714 treating constipation in a patient with 8,9-didehydro-N-demethyl-9-deoxo-6,11-dideoxy-6,9-epoxy-12-O-methyl-N-(1-methylethyl)-11-oxoerythromycin; unlike a laxative A compound of Formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents a C1-C6 alkyl group and R2 represents a C1-C6 alkyl group, while unlike a laxative, is effective in the treatment of constipation.
CN103301088A Chick embryo polysaccharide capsule preparation and preparation method thereof The invention relates to a chick embryo polysaccharide capsule preparation and a preparation method thereof. The chick embryo polysaccharide capsule preparation is a small-dosage medicinal preparation; each capsule contains 10mu g of chick embryo; the preparation contains the following auxiliary materials in percentage by weight: 95-99% of a filler, 0-10% of an adhesive and 0-5% of a lubricant. The preparation method comprises the steps of filling powder into the capsule directly and filling the powder into the capsule after being pelletized. The chick embryo polysaccharide capsule preparation provided by the invention is good in mobility, uniform in content, stable in preparation property, simple in production process and good in reproducibility, and can meet the requirements of large-scale industrialization.
CN103479627A Application of I-type acceptor antagonist of angiotensin II to promote hair growth The invention belongs to the technical field of medicines, and relates to a new application of a I-type acceptor antagonist of angiotensin II to promote hair growth. The I-type acceptor antagonist of angiotensin II has good hair growth promotion effect by creatively discovering, and research shows that the action mechanism on hair growth promotion is that: the I-type acceptor antagonist of angiotensin II is capable of exciting bradykinin B2 acceptor and causing release of prostaglandin F-2a, and thus local microenvironment is improved and hair growth is promoted through the prostaglandin acceptor approach; also, the I-type acceptor antagonist of angiotensin II is capable of effectively blocking the effecting of angiotensin II and promoting local blood supply, and thus the effect of promoting hair growth is realized. The application of the I-type acceptor antagonist of angiotensin II to promote hair growth provides excellent theory basis for development of multi-target medicaments, and provides a new direction for development of medicaments for treating various hair loss.
WO2013084182A1 Pharmaceutical composition that includes a pde4 enzyme inhibitor and an analgesic agent The present invention relates to a pharmaceutical composition that includes a phosphodiesterase-4 ("PDE4") enzyme inhibitor and an analgesic agent. Particularly, the present invention relates to a pharmaceutical composition that includes a benzofuropyridine compound as a PDE4 enzyme inhibitor and an analgesic agent, a process for preparing such composition and its use for the treatment of pain related disorder in a subject.
US7691848 10-[(2,2'-Dimethyl-1,1'-biphenyl-4-yl)carbonyl]-N-(3-methoxybenzyl)-10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-3-carboxamide; antifertility agents This invention provides pyrrolobenzodiazepine arylcarboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists, as well as pharmaceutical compositions and methods of treatment utilizing these compounds.
US20110003016 Hair care composition A hair treatment composition comprising a trichogenic material and an anti-dandruff agent.
CN102908520A Plaster for treating shingles by using polygonum perfoliatum The invention discloses a plaster for treating shingles by using polygonum perfoliatum. The weight ratios of the raw material components are as follows: 13 to 17 parts of polygonum perfoliatum, 4 to 8 parts of borneol, 6 to 10 parts of rhizoma coptidis, 4 to 8 parts of stephania tetrandra, 1 to 5 parts of rhizoma coptidis, 6 to 10 parts of violet, 6 to 10 parts of edible tulip, 13 to 17 parts of radix ilicis asprellae and 7 to 11 parts of blister beetle. In a formula provided by the invention, the borneol is capable of dredging collaterals and scattering stasis fire; the stephania tetrandra, the rhizoma coptidis, the polygonum perfoliatum and the rhizoma coptidis are capable of clearing away heat and toxic materials; and the edible tulip, the radix ilicis asprellae and the blister beetle are capable of attacking toxicity and dissolving stasis, so that the plaster is capable of effectively alleviating the pain of the patients suffering from shingles, remarkable in efficacy, low in toxic and side effects, and simple and feasible to operate.
WO2012047207A1 Compositions for treating chronic viral infections The present invention describes dietary compositions and methods of using such compositions to treat chronic viral infections, including hepatitis B and hepatitis C infections.
US20100280091 Tri-substituted 2-benzhydryl-5-benzylamino-tetrahydro-pyran-4-ol and 6-benzhydryl-4-benzylamino-tetrahydro-pyran-3-ol analogues, and novel 3,6-disbustituted pyran derivatives Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.
CN102526085A Pharmaceutical ointment for treating acne and preparation method thereof The invention relates to a pharmaceutical ointment for treating acne and a preparation method thereof. The pharmaceutical ointment for treating acne is made from stearic acid, glycerol, sodium bicarbonate, essences, ethanol, distilled water, metronidazole and erythromycin. During use, the ointment is directly applied to the affected area, and the active components are absorbed through pores to treat acne by directly killing bacteria in the local area, unclogging the pores and reducing the secretion of sebaceous glands. The clinical trials prove that the cure rate reaches more than 93% and no toxic or adverse effect occurs.
WO2014067417A1 Novel quinoline compound and use thereof The present invention relates to quinoline derivatives as represented by general formula I and pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein the substituents M, R1, R2, X, Y and n are as defined in the specification. The present invention also relates to the use of the compounds as represented by general formula I as a c-Met kinase inhibitor, and also relates to the uses of the compounds and pharmaceutically acceptable salt and hydrate thereof in the preparation of drugs for treating the diseases caused by the abnormally high expression of c-Met kinase, in particular to the uses thereof in the preparation of drugs for treating and/or preventing cancers.
EP1326599B1 Use of aivlosin for treating or preventing Lawsonia infections in pigs. The use of aivlosin, as much or as a pharmacologically acceptable (non-toxic) derivative such as an acid addition salt, for the preparation of a veterinary medicament for the treatment or prophylaxis of diseases and infections of pigs and poultry. In particular the diseases and infections treatable are necrotic enteritis in poultry and Lawsonia infections, Mycoplasma diseases and swine dysentery in pigs.
US20080057118 Divalproex pharmaceutical compositions Pharmaceutical compositions comprising a valproic acid drug compound, providing modified release of the drug.
WO2011112956A1 Agonist/antagonist compositions and methods of use The present invention relates to novel compositions comprising an agonist and an antagonist, in certain ratios which allow for the onset of agonist action followed quickly by alleviation by antagonist action, and methods of use in personal defense and law enforcement.
WO2013068993A3 Tyrosine isomers as therapeutic agents The present invention relates to prevention or treatment of diseases related to abnormal cell proliferation, such as cancer, by administering meta- or orto-tyorosine to a subject in need thereof, for instance a human subject. More specifically, the present invention provides isomers of tyrosine for its use in the prevention or treatment of a disease and in the preparation of pharmaceutical compositions, methods of for treating or preventing diseases, such as cancer and cancer metastases, and pharmaceutical compositions containing meta- and/or orto-tyorosine.
CN1611213A Novel 13 uses of neoarsphenamine The present invention discloses new application of neoarsphenamine. Said neoarsphenamine has the specific effect for curing the following 13 diseases: 1. rheumatoid arthritis; 2. various neuralgias of sciatica and intercostal neurolgia, etc. 3 angiitis; 4. leukemia; 5. psoriasis; 6 gonorrhea; 7 herpes zoster; 8. osteomyelitis and myelitis; 9 erysipelas; 10. nascsinusitis and frontal sinustits; 11. viral cold and viral ophthalmia; 12. eczema; and 13. carbuncle and cellulitis.
WO2008157205A2 Methods and compositions for treating urinary tract infections using agents that mimic or elevate cyclic amp Methods and compositions are provided for treating a urinary tract infection (UTI). The methods involve administering to a subject in need thereof a cAMP elevator or agent that mimics cAMP, particularly a labdane diterpene such as forskolin or a derivative or analog thereof in a therapeutically effective amount to treat a UTI. The methods may further include administration of at least one cAMP elevator in combination with one or more additional active compounds from other classes of therapeutic agents, such as antimicrobial agents or cholesterol lowering drugs. Compositions of the invention include pharmaceutical compositions and kits for treating a UTI in a subject in need thereof that include therapeutically effective amounts of at least two cAMP elevators, particularly where one of the cAMP elevators is a labdane diterpene such as forskolin or a derivative or analog thereof. In particular, the compositions and kits may also include at least one cAMP elevator in combination with one or more additional active compounds from other classes of therapeutic agents, such as antimicrobial agents or cholesterol lowering drugs.
US7390922 Phenolic acid salts of gabapentin in liquid and/or semi-solid dosage forms and methods of use The present invention relates to pharmaceutical compositions of gabapentin tannate, processes for production of those compositions and methods of use of those compositions. The present invention provides a novel process for preparation of the tannate salt of gabapentin in liquid or semi-solid dosage form for human and veterinary pharmaceutical use. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. The process may utilize either natural or synthetic tannic acid.
WO2009012075A1 Use of iop-lowering agents for treating primary and secondary forms of glaucoma Methods and compositions for controlling ocular hypertension associated with (i) primary open angle glaucoma (POAG), (ii) other forms of glaucoma, or (iii) glucocorticoid therapy are disclosed. The methods involve administration of angiostatic agents and other IOP-lowering agents via local injections in the anterior segment of the eye. The most preferred IOP-lowering agents are angiostatic steroids, particularly anecortave acetate, and the most preferred route of administration is an anterior juxtascleral injection or implant. The invention is based in part on the discovery that anterior juxtascleral injections of anecortave acetate are capable of controlling intraocular pressure for sustained periods of from one to several months or more. This result is believed to be attributable to facilitation of access of the anecortave acetate to the trabecular meshwork via the anterior juxtascleral route of administration. This route of administration is also believed to be advantageous for other types of IOP-lowering agents, particularly molecules that cannot readily penetrate the cornea due to size or other physical properties.
CN102552392A Nursing product for protecting fingers of diabetics The invention relates to a nursing product for protecting fingers of diabetics. The nursing product contains the following rare medicinal materials of: mint oil, rana temporaria oil, royal jelly, bee glue, borneol and the like. The nursing product has the effects of softening skin and stopping bleeding, and can be used for injection, phlebotomization, infusion, blood collection, acupuncture and moxibustion and the treatment of wounds of trauma.
CN101002802A Medicine for treating wound and ulcer, and its preparing method A medicine in the form of powder for treating sore and ulcer is proportionally prepared from Chinese gall, gentamycin, metronidazole, and anisodamine and zinc gluconate through baking Chinese gall, proportionally mixing it with others, grinding, sieving, sterilizing and packing.
EP2442803A1 Modulation of systemic exposure to rifaximin The present invention relates to the effect of hepatic insufficiency on the pharmacokinetics of rifaximin. Also provided are methods of determining an appropriate dose of rifaximin for a subject suffering from hepatic insufficiency. In addition, methods of treatment are provided subjects having or susceptible to hepatic insufficiency to be treated with rifaximin.
CA2356212C Crystalline bis[(e)-7- [ 4-(4- fluorophenyl)- 6-isopropyl-2- [methyl (methylsulfonyl) amino] pyrimidin -5-yl] (3r,5s)-3, 5-dihydroxyhept -6-enoic acid]calcium salt The present invention relates to a crystalline form of the compound bis[(E)-7-[ 4-(4- fluorophenyl)- 6-isopropyl-2- [methyl (methylsulfonyl) amino] pyrimidin-5-yl] (3R, 5S)-3, 5-dihydroxyhept -6-enoic acid]calcium salt, as well as processes for its manufacture and pharmaceutical compositions comprising the crystalline form, which is useful as an agent for treating hyperlipidemia, hypercholesterolemia and atherosclerosis.
CN102131799A Method for splitting omeprazole salts The invention relates to a method for splitting potassium salts of racemic omeprazole by preferable crystallization, wherein said potassium salts of racemic omeprazole is a solvate of ethanol and/or ethyleneglycol. The method comprises the step of transforming the omeprazole into a potassium salt in the form of a solvate or a mixture of these solvates in the presence of an excess of a inorganic base defining a potassium source, said potassium salts being in the form of conglomerates, and splitting said conglomerates independently or simultaneously by preferable crystallization for separating the two enantiomers (S) and (R) of the potassium salts from the omeprazole.
CN101822796A Silver ice buccal tablet, and preparation method and application thereof The invention relates to a silver ice buccal tablet, and a preparation method and application thereof. The silver ice buccal tablet disclosed by the invention is a tablet which is prepared by extract prepared by taking 120 parts of honeysuckle flower, 17 parts of radix glycyrrhizae preparata, 25 parts of katsumade galangal seed and 12 parts of indigo woad root as raw materials, 5 parts of zinc gluconate, 1.25 parts of menthol, 5 parts of borneol and 430-450 parts of auxiliary materials, wherein in the auxiliary materials, the ratio of microcrystalline cellulose and mannitol is 1:2-20. The invention solves the problems of stability and large-scale production of the silver ice buccal tablet by improving the auxiliary materials and the preparation technique.
EP1888587A1 2-amido-6-amino-8-oxopurine derivatives as toll-like receptor modulators for the treatment of cancer and viral infections, such as hepatitis c This invention relates to purine derivatives, to processes for their preparation, to compositions containing them and to their use. The present invention provides compounds of formula (I) wherein R1, R2, R3, R9, R9a and Y are defined in the description. More particularly, the present invention relates to the use of purine derivatives in the treatment of a variety of viral infections and immune or inflammatory disorders, including those in which the modulation, in particular agonism, of Toll-Like Receptors (TLRs) is implicated. Accordingly, the compounds of the invention are useful in the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infections, inflammatory diseases such as asthma and arthritis, and cancer.
US20130089627 Method for treating a cancer caused by cancer stem cells This invention provides a method for treating a cancer caused by cancer stem cells in a subject in need thereof, comprising administering to the subject an effective amount of Antrodia camphorata extracts. The invention also provides a method for treating a cancer caused by cancer stem cells in a subject in need thereof, comprising administering to the subject an effective amount of 4-acetyl-antroquinonol B.
US20080090799 2-pyridinecarboxamide derivative having gk-activating effect Compounds of a formula (I) and their pharmaceutically-acceptable salts are disclosed. The compounds have glucokinase-activating effect and are therefore useful for treatment of diabetes and obesity. R1 and R2 each independently represent a lower alkyl group; X1 represent a group of a formula (II-1): wherein: R11 and R12 each independently represent a hydrogen atom or a lower alkyl group, or taken together with the nitrogen atom to which they bond, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring (one carbon atom constituting the 4- to 7-membered nitrogen-containing aliphatic ring may be replaced by an oxygen atom), or taken together with a carbon atom in (CH2)m, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring; m indicates an integer of from 1 to 3.
US20060121041 Gpcs as modifiers of the irrtk p21 pathways and methods of use Human GPC genes are identified as modulators of the IRRTK or p21 pathways, and thus are therapeutic targets for disorders associated with defective IRRTK or p21 function. Methods for identifying modulators of IRRTK or p21, comprising screening for agents that modulate the activity of GPC are provided.
US20100029712 Irrigation solution and method for inhibition of pain, inflammation, spasm and restenosis A method and solution for perioperatively inhibiting a variety of pain, inflammation, spasm and restenosis processes resulting from cardiovascular or general surgical, therapeutic and diagnostic procedures. The solution preferably includes multiple pain and inflammation inhibitory agents, including at least one local anesthetic agent, and spasm inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. Specific preferred embodiments of the solution of the present invention for use in cardiovascular and general vascular procedures also include anti-restenosis agents.
US20110045089 Vitamin k3 derivative / nsa formulation The present invention discloses highly stabilized nicotinamide (NA) formulated vitamin K3 derivative particles, whereby the NA forms a physical protective layer (both continuous and discontinuous) leading to highly stabilized vitamin K3 derivative particles, as well as a process for their production.
US20110262465 Prostate stem cells and uses thereof Prostate stem cells and prostate cancer stem cells and their use in treating prostate cancer and regenerating prostate tissue are disclosed.
EP2396407A1 C-cbl and antagonists thereof for the treatment and diagnosis of cancer The present invention relates to the treatment of cancer. More specifically, the present invention relates to the use of c-cbl as a marker for the diagnosis and/or prognosis of cancer, and to the use of a c-cbl antagonist for the treatment of a cancer associated with resistance to apoptosis.
WO2014069401A1 Pulmonary disease-specific therapeutic agent The purpose of the present invention is to provide a pulmonary-specific therapeutic agent that can be intravenously administered. Provided is a pulmonary-specific therapeutic agent characterized by containing sustained release microspheres that contain a medicinal compound and being intravenously administered.
WO2013148114A1 P300/cbp inhibitors and methods of use The subject invention pertains to a class of compounds that inhibit the function of p300/CBP, GCN5 and PCAF. P300/CBP inhibition was noted to result in inhibition of tumor cell growth and killing of tumor cells. P300/CBP inhibition is, thus, useful for treatment of various types of cancers, including acute lymphoblatic leukemia (ALL), acute myelogenous leukemia (AML), acute promyelocytic leukemia, chronic lymphocytic leukemia (CLL), chronic myelogenous leukemia (CML), acute monocytic leukemia (AMOL), hairy cell leukemia, large cell immunoblastic lymphoma, plasmacytoma, multiple myeloma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, leukemia, brain cancer, lung cancer, central nervous system (CNS) cancer, melanoma, renal cancer, prostate cancer, colon cancer, ovarian cancer and breast cancer. The compounds disclosed herein can be used alone or in combination with other cancer treatment regimens (e.g., radiation therapy and/or other chemotherapeutic agents that are administered to a subject having a tumor, cancer or neoplasia).
US7033606 Pharmaceutical composition intended in particular for the prevention and the treatment of radiomucositis and chemomucositis The invention concerns a pharmaceutical composition designed to adhere to a mucous membrane for preventing or treating radiotherapy-related and chemotherapy-related mucositis, induced by radiotherapy or combined radiochemotherapy, comprising an effective amount of an antiradical compound mixed with a vehicle, which is liquid at room temperature and gels at the mucous membrane temperature and capable of adhering to the mucous membrane by its gelled status.
US20050221347 Inhibitors of binding between proteins and macromolecular ligands Disclosed is a compound which inhibits binding between a target protein and a macromolecular ligand of the target protein. The compound comprises a targeting group, an attaching group and, optionally a linker group. In one aspect of the invention, the targeting group is a moiety that binds non-covalently to a surface of the target protein with a Kd of greater than about 0.1 μM and within sufficient proximity to the target protein/macromolecular ligand binding site to inhibit binding between the target protein and the macromolecular ligand. In another aspect of the invention, targeting group is degradable in vivo. In yet another aspect of the invention, the compound comprises a linker group that is cleavable in vivo.
US20130059886 Polymorphic form of fexofenadine hydrochloride, intermediates and process for its preparation The present invention relates to a novel polymorphic form of Fexofenadine hydrochloride, to a process for preparing it, to pharmaceutical compositions containing it, as well as its use. The invention also relates to intermediates useful for the preparation of Fexofenadine hydrochloride, antihistamine drug used in the treatment of allergy symptoms.
EP2644624A1 6-deoxy-6-thioether-amino acid cyclodextrin derivatives and preparation method thereof 6-deoxy-6-thioether-amino acid cyclodextrin derivative is obtained by condensing an amino acid derivative with halogenated cyclodextrin in presence of alkali. The 6-deoxy-6-thioether-amino acid cyclodextrin derivative includes 6-deoxysulfinyl-6-thioether-amino acid cyclodextrin derivative and 6-deoxysulfonyl-6-thioether-amino acid cyclodextrin derivative. Compounds provided are for reversing neuromuscular relaxation in patients and animals induced by muscular relaxants. The compounds are able to rapidly reverse and antagonize muscular relaxation induced by muscular relaxants and can be administrated in preparing a drug having an antagonist effect on muscular relaxation. The compounds have low production cost and are able to reverse and antagonize a wide rage of muscular relaxations, thus effectively broaden scope of clinical use. More importantly, the compounds have a safe dose at least doubled compared to prior arts. The compounds have a general formula (I).
WO2010138725A1 Treatment of pancreatic cancer using a dr5 agonist in combination with gemcitabine Methods and compositions for treatment of exocrine pancreatic cancer in a human patient comprising administering a therapeutically effective amount of a DR5 agonist and gemcitabine. Methods and compositions for treating a patient by identifying the alleleic variant of FcγRIIIA.
CN101874885A Method for preparing Mongolian medicament preparation The invention discloses a method for preparing a Mongolian medicament preparation, and particularly relates to a method for preparing a Mongolian medicament preparation for treating hyperplasia of mammary glands. The method comprises the following steps of: grinding 23 Chinese medical herbs in the formula such as leonurus into 60-mesh fine powder, decocting the powder for extraction, extracting the decoction by ethanol, mixing the decoction concentration solution and the ethanol extraction concentration solution, and using the mixed solution as an excipient; and grinding 7 kinds of Chinese medical herbs in the formula such as Chinese caterpillar fungus into 120-mesh fine powder, adding the concentration solution into the fine powder for rapping screening pill moulds, preparing the pill moulds into pills by using water, and performing drying, screening, vermilion coating, polishing, drying, radiation sterilization and packaging to obtain the finished product. The medicament preparation prepared by the technical scheme has the advantages of meeting regulations of National Formulary, having an effect of treating hyperplasia of mammary glands and providing a safe and effective therapeutic medicament for patients suffering from hyperplasia of mammary glands.
WO2007081871A1 Therapeutic salt compositions of sulfonyl ester prodrugs of proton pump inhibitors and methods for their preparation Method for preparing a salt of the following sulfonyl ester prodrugs of proton pump inhibitors the compositions and the dosage forms thereof are disclosed herein.
US20110229437 Method of Treating Asthma with Antiviral Agents The present invention provides a method of treating asthma by administering a therapeutically effective amount of an antiviral agent to a patient. The antiviral agent may be a neuraminidase inhibitor, a viral fusion inhibitor, a protease inhibitor, a DNA polymerase inhibitor, a signal transduction inhibitor, a nucleoside reverse transcriptase inhibitor (NRTI), a non-nucleoside reverse transcriptase inhibitor (NNRTI) or an interferon. The antiviral agent may be administered to the patient by inhalation, nasally, intravenously, orally, subcutaneously, intramuscularly or transdermally. For example, the antiviral agent may be formulated for delivery as aerosols to the patient.
US20110098325 Pyridine benzamides and pyrazine benzamides used as pkd inhibitors The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyridine benzamide and pyrazine benzamide compounds (referred to herein as PDBA and PZBA compounds) which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD, that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc.
EP2283838A2 Docosahexaenoic acid for treating subclinical inflammation This invention is directed to methods and compositions which impede the development and progression of diseases associated with subclinical inflammation. Subclinical inflammation is commonly associated with atherosclerotic cardiovascular disease, coronary disease or cerebrovascular disease. The methods and compositions of the invention are also particularly suited to providing therapy for subclinical inflammation in diabetic and prediabetic patients. Methods of the invention comprise administration of DHA alone and in combination with antiplatelet drugs.
CN101524140A Application of vanadium-rich eggs and method for producing same The invention discloses vanadium-rich eggs for treating diabetes mellitus and a method for producing the same, and is characterized in that the vanadium-rich eggs are cooked for eating, and the method for producing the vanadium-rich eggs is to add 30 to 200 ppm of vanadium to the basic ration for laying hens to eat freely, and collecting laid eggs which are the vanadium-rich eggs. The vanadium added to the basic ration for the laying hens can be one or more of VOSO4, NH4VO3, NaVO3, Na3VO4, vanadium organic complex, and the like, and the vanadium in the eggs has better biocompatibility, and has better curative effect and smaller toxicity compared with inorganic vanadium and organic vanadium.
CN1762347A Andrographolide preparation and its production method The invention discloses an andrographolide and preparation its preparing method, which can be used mainly for treating common cold, throat pain, aphtae, dysentery, and cerebrovascular diseases.
US20110028504 Formulation of radioprotective alpha beta unsaturated aryl sulfones A pharmaceutical composition is provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject. An effective amount of the pharmaceutical composition provided comprising an effective amount of at least one radioprotective α, β unsaturated aryl sulfone, and at least one component selected from the group consisting of a) at least one water soluble polymer in an amount between about 0.5% and about 90% w/v, b) at least one chemically modified cyclodextrin in an amount between about 20% and about 60% w/v, and c) DMA in an amount between about 10% and about 50% w/v.
US20080050454 Mixture of vitamins, minerals; for physiologically stressful states as pregnancy, lactation, nutritional deficiencies; nutraceuticals The present invention relates to compositions that may be swallowable, chewable or dissolvable, comprising various vitamins and minerals, and in a specific embodiment comprising vitamin A, beta carotene, B-complex vitamins, vitamin C, vitamin D3, vitamin E, iron, magnesium and zinc, and methods for using these compositions for nutritional supplementation in subjects undergoing physiologically stressful events, such as, for example and without limitation, pregnancy, lactation or any disease state.
CN103705497A Application of liothyronine in preparation of medicine for treatment or prevention of influenza virus infection The invention discloses an application of liothyronine in preparation of a medicine for prevention or treatment of influenza virus infection. Reports related to liothyronine resistant to influenza viruses are unavailable so far. Liothyronine with completely non-toxic concentration is selected for an antiviral experiment, and a result shows that the small molecular compound has significant antiviral activity and is in dose-dependent association. Then, the antiviral activity of liothyronine to different types and subtypes of influenza viruses is detected, and a result shows that liothyronine can inhibit replication of all detected viral strains and has a dose dependent effect, thereby representing that the anti-influenza virus activity of liothyronine has a certain broad spectrum. Therefore, liothyronine can be used as a novel anti-influenza virus medicine for development, and provides a novel way and means for treating influenza.
US7687507 Protein tyrosine kinase, such as Janus Kinase 3, inhibitors, immunosuppressants; organ transplants, lupus, multiple sclerosis, psoriasis; antidiabetic agents, antiarthritic agents, anticarcinogenic agents, Alzheimer's Disease, Crohn's Disease, Inflammatory Bowel Disease, autoimmune thyroid disorders A compound of the formula wherein R1, R2 and R3 are as defined above, which are inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.
CN101780049A Enteric solid preparation using feinuobeite acid and feinuobeite salt as major ingredients and preparation method thereof The invention provides an enteric solid preparation using feinuobeite acid and feinuobeite salt as major ingredients and a preparation method thereof. The invention relates to an enteric solid preparation using feinuobeite and feinuobeite salt or feinuobeite hydrate as active ingredients and a preparation method thereof. The invention aims at providing a novel preparation of feinuobeite and feinuobeite salt for a large number of patients and medical personnel, and the novel preparation of feinuobeite and feinuobeite salt fully exerts the medicine curative effect, reduces the adverse effect, is convenient for children and old people to take in a decrement way, is convenient to carry, store and transport, and is suitable for large-scale production. The invention uses the feinuobeite and the feinuobeite salt or the feinuobeite hydrate as the active ingredients, some accessory ingredients of specified types are proportionally added into the ingredients for being prepared into enteric grains or pellets according to the process provided by the invention, and the ingredients can be further prepared into dry suspension preparations, capsules or tablets.
CN103156838A Medicinal application of chromone compound The invention discloses new application of a chromone compound KY12 in preparation of a targeted anti-tumor medicament. Experimental results show that the compound KY12 can selectively kill tumor cells with tumor specific mutant genes p53 and Ras under the concentration which is nontoxic for wild normal mouse embryo fibroblasts, namely the compound has application potential for preparing the personalized treatment medicament for the tumor specific mutant genes p53 and Ras.
CN1977831A Inclusion cyclodextrin/vanillin ex polar bear medicinal composition and its preparing method The present invention relates to an inclusion type cylodextrin/vanillin medicine composition. It is characterized by that the mole ratio of cyclodextrin and vanillin is 1:0.2-1, its inclusion constant Ka is 1933M-1-7471M-1. The cyclodextrin of optimum scheme adopts beta-cyclodextin or hydroxypropyl-beta-cyclodextrin or sulfobutyl-beta-cyclodextrin or mixture of beta-cyclodextrin and hydroxyprobyl-beta-cyclodextrin or mixture of beta-cyclodextrin and sulfobutyl-beta-cyclodextrin. Its preparation method includes the following steps: mixing beta-cyclodextrin with pure water to obtain suspension, adding vanillin of 0.5 mole ratio, grinding them, cooling and standing still for 10 hr, press-filtering and drying so as to obtain the solid inclusion product.
WO2005058321A1 USE OF METABOTROPIC GLUTAMATE RECEPTOR 5 (mGLuR5) ANTAGONISTS FOR THE TREATMENT OF GASTROINTESTINAL DISORDERS. The present invention relates to the use of metabotropic glutamate receptor 5 (mGluR5) antagonists for the treatment of functional gastrointestinal disorders, such as functional dyspepsia.
WO2014022858A1 Enzyme-activating compounds and compositions The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
CN101152199A Health care food for improving sexual function of men and women The invention discloses a health food used to improve sexual functions of both male and female. The health food contains the following weight percentage of components: 30 to 50 portion of L-arginine, 6 to 10 portion of icariin, 3 to 6 portion of Fructus Tribuli and 5 to 15 portion of taurine. After lots of animal and human body function tests, the health food of the invention used to improve sexual functions of both male and female causes no side effects after long term of consumption, has good tolerance without changing hormone balance of human body.
WO2007030618A2 Bicyclic derivatives as modulators of voltage gated ion channels Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.
US20100267720 Crystalline Forms of 2-Hydroxy-3- [5- (Morpholin- 4- Ylmethyl) Pyridin-2-YL] IH- Indole- 5 -Carbonitrile Citrate The present invention relates to new crystalline forms of 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile citrate, a Form D and a Form E, respectively, a process for their preparations, pharmaceutical formulations containing said compounds and to the use of said active compounds in therapy, and particularly to GSK3 related conditions and disorders.
CN103435545A Tetrahydroisoquinoline quaternary ammonium salt derivatives as well as preparation method and analgesia application thereof The invention belongs to the field of medicinal chemistry and particularly relates to tetrahydroisoquinoline quaternary ammonium salt derivatives, a composition containing the derivatives, as well as application of the derivatives or the composition as a k-opioid receptor antagonist in the analgesia aspect. Proved by a pharmacodynamic experiment, the compound disclosed by the invention has an analgesia function but has no side effect of central sedation and anxiety which are common in the medicaments.
CA2727935A1 Preparation of controlled release skeletal muscle relaxant dosage forms The present invention is directed to a method of preparing an extended release pharmaceutical composition com-prising cyclobenzaprine, comprising coating inert particles with a cyclobenzaprine-containing a drug layering composition to form I R beads, then coating the I R beads with an extended-release coating to form E R beads.
WO2013144079A1 4-oxo-2-pentenoic acid and skin pigmentation The present invention relates generally to the field of enhancing skin appearance. One aspect of the invention aims to provide a composition comprising 4-oxo-2-pentenoic acid for use in the reduction or prevention of regions of the skin with darker pigmentation. The present invention also relates to cosmetic use of a composition comprising 4-oxo-2-pentenoic acid for the reduction or prevention of regions of the skin with darker pigmentation.
CN103751146A Vitamin E softgel and preparation method thereof The invention relates to a vitamin E softgel and a preparation method thereof. The vitamin E softgel comprises content and a capsule casing. The content comprises, by weight, 10-60% of natural vitamin E and 40-90% of soybean oil. Compared with the prior art, the vitamin E softgel has the advantages of high safety, good absorbency and strong pertinence.
WO2009137966A1 A inhibitor for depressing the absorption of sucrose The present invention discloses a new inhibitor for depressing the absorption of sucrose, wherein the inhibitor is arabinose complexes of trace element which frequently occurs in the body. The effect of the complexes is same whenever alone or combined with other natural product. The complexes can decrease the level of blood sugar and reduce weight. The present invention also provides a convenient method for separating arabinose.
WO2012112919A1 Stromal derived factor inhibition and cxcr4 blockade The invention relates to inhibition of SDF-la expression in subacromial bursa cells by CXCR-4 inhibitors. Bursal cell migration in response to SDF-α stimulation is also decreased in the presence of CXCR4 inhibitors. Accordingly, provided are methods for treating or ameliorating a musculoskeletal disorder.
US20100074970 Method and composition for preventing and healing osteonecrosis of the jaw A method and composition for preventing and treating all forms of osteonecrosis of the jaw are disclosed. The composition is comprised of 0.005%-2.0% weight/volume (w/v) chlorine dioxide source, such as sodium chlorite, chlorite ion, stabilized chlorine dioxide or similar and may take the form of a paste, gel, rinse, spray, powder, varnish or similar. The method for treatment and prevention includes the application of the composition in the oral cavity and other body areas affected by osteonecrosis of the jaw.
WO2010057443A1 Use of 9,10-anthraquinone compounds Use of 9,10-anthraquinone compounds of formula (I) or pharmaceutical salts thereof or plant extracts containing said compounds in the preparation of anti-HCV medicaments is disclosed, in which Y1 are Y2 are independently hydrogen, hydroxyl or groups of formula (II); and R1, R2, R3, R4, R5 and R6 are independently hydrogen, hydroxyl, carboxyl, cyano group, nitro group, groups of formula (III) or groups selected from those substituted or unsubstituted groups: amino, C1-C6 aliphatic hydrocarbon, C3-C7 cyclic aliphatic hydrocarbon, C1-C6 alkoxy, C2-C7 carbalkoxy, C1-C4 acyloxy, C6-C20 aryl, or 5 to 7 members heterocyclic or benzoheterocyclic thereof; or R5 and R6 form the group of formula (IV). The compounds of present invention are cheap, safe and effective because that they mostly come from traditional Chinese medicines and have better anti-HCV effects and lighter side effects.
US20100016409 Rna Nanoparticles and Nanotubes The instant invention provides polyvalent RNA nanoparticles comprising RNA motifs as building blocks that can form RNA nanotubes. The polyvalent RNA nanoparticles are suitable for therapeutic or diagnostic use in a number of diseases or disorders.
WO2009145841A1 Compositions and methods for immunotherapy The present invention provides novel immunotherapeutic compositions and methods useful for treating or preventing microbial infections, weakened immune systems, diseases in which cells have become obligately anerobic and cellular proliferative disorders including cancer. The immunotherapeutics herein use benzaldehyde derivatives, precursors and intermediaries alone or in combination with additional therapeutic agents to stimulate the immune system and inhibit cellular proliferation. The immunotherapeutics of the present invention are particularly useful in the treatment of microbial infections and cellular proliferative disorders which are resistant to traditional methods of treatment such as antibiotics and chemotherapy.
US20100112076 Gellan-Gum Nanoparticles and Methods of Making and Using the Same Compositions containing a reaction product of gellan gum and polyethylene glycol are disclosed. Methods of making controlled-release gellan gum nanoparticles and methods of using controlled-release gellan gum nanoparticles are also disclosed.
WO2007021061A1 Composition comprising oleic acid and the use thereof The present invention relates to the pharmaceutical composition and health care food comprising oleic acid having neuroprotective activity. The oleic acid of the present invention has potent neuroprotective effect and recovery effect on neurological behavior. Therefore, it is useful as the therapeutics for the prevention or treatment of degenerative brain diseases in human or mammal.
US7989444 Compounds having affinity for dopamine D3 receptor and uses thereof Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.
US20110189292 Dermal fillers comprising silk fibroin hydrogels and uses thereof The present specification provides compositions useful as dermal fillers and methods using such compositions to treat a condition of skin.
WO2005103017A1 Method for increasing specific surface area of slightly soluble drug A method for preparing a powder being improved in the rate of dissolution, characterized in that it comprises converting a slightly soluble drug having an acidic group (for example, 3-(5-{2-[5-methyl-2-(4-methylphenyl)-1,3-oxazole-4-yl]ethoxy}3,4-dihydronaphthalene-1-yl)propanoic acid and the like) to a solution of a metal salt thereof, and then neutralizing the solution to thereby precipitate the drug. The above method allows the preparation of a powder being increased in its specific surface area and improved in the rate of dissolution, and thus is markedly useful as a method for the production of a raw powder of a drug.
CN1736372A Compound amino acid for injection and its preparation process The invention relates to medicinal compound amino acids for injection and the preparing process, wherein the formulation comprises eighteen kinds of amino acids freeze-dried powder, as well as excipient, auxiliary solvent, pH modifier, stabilizing agent for oxidation resistance and metal chelating agent.
CN101062012A Narcotic analgesics injection liquid The invention discloses a narcous analgetics injection in medicinal domain, which is characterized by the following: allocating 1-20000milligram sedative-hypnotic imidazole, 1-50000milligram narcous analgetics and 1000mL injection water; getting the product. This product possesses sedative and analgesic function, which can decrease the cost of patient.
US20120269738 Imaging Beta-Amyloid Peptides and Inhibition of Beta-Amyloid Peptide Aggregation The present invention relates to methods of detecting and monitoring aggregation of beta-amyloid peptides which are associated with neurodegenerative diseases as well as treating and/or preventing the neurodegenerative diseases by using carbazole-based fluorophores. In particular, the present invention provides methods for labeling and imaging the beta-amyloid (Aβ) peptides, oligomers, and fibrils in vitro and/or in vivo, as well as treating and/or preventing Alzheimer's disease by using the carbazole-based fluorophores of the present invention.
EP1589970A2 Pharmaceutical compositions comprising thieno [2,3-c]pyridine deritives and use thereof The present invention provides thieno[2,3-C]pyridine derivatives, pharmaceutical compositions comprising the thieno[2,3-C]pyridine derivatives, and methods of use thereof. The compounds capable of inhibiting glycosaminoglycan (GAG) interactions with effector cell adhesion molecules (ECAM) are useful for treating diseases and disorders mediated by GAG-ECAMs interactions, particularly inflammatory and autoimmune diseases, viral diseases, cancer, and amyloid disorders.
WO2009124103A2 Combination therapies comprising par1 antagonists with par4 antagonists The present invention is directed to a pharmaceutical composition comprising an effective amount of at least one PAR1 antagonist, at least one PAR4 antagonist, optionally, an effective amount of at least one cardiovascular agent, and, optionally, a pharmaceutically acceptable carrier. The present invention also provides for the use of theses pharmaceutical compositions to treat various diseases associated with thrombosis.
CA2658361A1 Ophthalmic formulations for the treatment of inflammation The invention relates to methods of treating mucositis comprising administering a compound of formula A, compound of any one of formulae 1 to 46, lipoxin compound, or oxylipin compound.
EP1702621A2 Metal/Thiol biocides A composition is described wherein metal is chelated by a complexing agent such as a pyrithione or certain other thiol compounds in the form of a metal complexing agent complex, wherein the metal is selected from the group consisting of bismuth, arsenic and antimony. Methods for using the composition as a bacteriocidal, bacteriostatic, antibiofilm, antifungal, and antiviral agent and as a disinfectant and preservative are also provided.
CN1931247B Medicine for treating rhinitis and its preparation process The present invention discloses one kind of medicine for treating rhinitis, and the medicine is prepared with centipeda herb 100-500 weight portions, rhubarb 50-300 weight portions, lily magnolia 50-300 weight portions, cocklebur fruit 50-300 weight portions, mint 50-300 weight portions and borneol 1-10 weight portions. The medicine has obvious systemic and local antiallergic effect and antiphlogistic effect, and is used in treating allergic rhinitis, chronic rhinitis, etc. It has fast acting, determined curative effect, high safety and less toxic side effect. The present invention also discloses the preparation process of the medicine.
US20080008773 Food beverage or feed for the promotion of osteogenesis comprising umbelliferae, liliaceae or compositae plant species The present invention relates to a therapeutic agent or prophylactic agent for a disease requiring promotion of osteogenesis or enhancement of bone morphogenetic protein production, an agent for promotion of osteogenesis or an agent for enhancement of bone morphogenetic protein production, and a food, beverage or feed for promotion of osteogenesis or enhancement of bone morphogenetic protein production, characterized in that each comprises as an effective ingredient a processed product derived from a plant. Also, the present invention relates to a method for measuring an enhancing action for bone morphogenetic protein production, a method for screening a substance having an enhancing action for bone morphogenetic protein production, and a method for preparing a substance having an enhancing action for bone morphogenetic protein production, each method using a specified cell.
US20090036449 Indazolesquaric Acid Derivatives as Chk1, Chk2 and Sgk Inhibitors Novel squaric acid compounds of the formula (I), in which R, R1, R2, R2′, R2″, R3, B, B′ and X have the meanings indicated in Claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be used for the treatment of diseases and complaints such as cancer, diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.
CN103316314A Muscle and bone joint dredging paste The invention discloses muscle and bone joint dredging paste. The muscle and bone joint dredging paste comprises water, propylene glycol, mineral oil, mineral ester, cetostearyl alcohol, glyceryl stearate, polysorbate-60, sea buckthron oil, laurocapram, cinnamon oil, turpentine, clove oil, safflower extract, borneol, pseudo-ginseng extract, mint leaf oil, ginger root oil, pepper powder, capsicine, bisabolol and bis(hydroxymethyl)imidazolidinyl urea. The muscle and bone joint dredging paste can be prepared simply, has obvious effects, can be smeared on parts such as human body joints, muscle body and ligament, can produce effects of loosening and nursing, and can keep a human body health by improving a movable capability of skin and joints.
CN102600169A Application of compound mosapride in preparing information therapeutic medicament as well as preparation method thereof and novel medicine prepared by using compound The invention discloses an application of compound mosapride in a preparing information therapeutic medicament as well as a preparation method thereof and a novel medicine prepared by using the compound. The information therapeutic medicament is not directly contact with a human body during treatment, the substance element of the medicament is not consumed, the medicament information is only utilized for physiotherapy, the effect of chemotherapy is achieved, the treatment windows are expanded by more than thousand times, and the side effects of the chemotherapy are avoided. The mosapride is used as the information therapeutic medicament, the content of an active ingredient is not changed, and the information therapeutic medicament can be effectively used as a chemotherapy general preparation for secondary use.
CN102827131A Isoflavone carbamate compound, preparation method and applications of isoflavone carbamate compound The invention discloses a novel isoflavone carbamate compound (I) and a pharmaceutically acceptable salt of the isoflavone carbamate compound, and also discloses a preparation method of the compound and applications in the preparation of drugs for treating and/or preventing related neurodegenerative diseases, wherein the diseases include but not limit to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, human immunodeficiency virus (HIV) related dementia, multiple sclerosis, progressive lateral sclerosis, neuropathic pain, glaucoma and the like.
EP2537520A1 Hepatics C therapies The invention provides methods for treating hepatitis C viral infections and related viral infections, as well as compounds and compositions that are useful for treating such infections
US20090004137 Uridine Derivatives as Antiviral Drugs Against a Flaviviridae, Especially Hcv The invention relates to the use of an uridine derivative of formula (I); wherein —R1 represents monohalogenated alkynyl or dihalogenated alkenyl; —R2 is chosen from among hydrogen, hydroxyl, O-alkyl, O—CO alkyl and halogen; —R3 is chosen from among hydrogen, hydroxyl, O-alkyl, O—CO alkyl, halogen, SH, S-alkyl and N3; and —R4 is chosen from among hydroxyl, O-alkyl, O—CO alkyl, O-phosphate, O-diphosphate, O-triphosphate and O phosphonate, as well as its possible tautomers, its possible pharmaceutically acceptable addition salts with an acid or a base, and its N-oxide forms, for the preparation of a drug having antiviral activity against a Flaviviridae.
EP1002082B1 Transcriptional silencer protein nrf NRF is a novel inhibitory transcription factor binding to specific DNA sequences and silencing transcriptional activity of proximal DNA-binding activators, e.g. NF-KB binding sites. NRF is a modulator protein of NF-KB family members controlling genes of significant biomedical importance such as those encoding inflammatory cytokines, MHC proteins, cell adhesion molecules, and viruses. Based on this it represents a molecular target in the development of novel anti-inflammatory therapies for a variety of pathologic disorders such as ischemia, hemorrhagic and septic shock, allograft rejection, bacterial meningitis, acute airway inflammation and the pulmonary complications induced by cardiopulmonary bypass. Furthermore, this might apply for certain cancers and other diseases. NRF as a target for drugs (obtained e.g. by IITS) is protected. Agonists as well as antagonists of NRF are also protected. Further applications such as the use of NRF protein and its fusion proteins or NRF DNA sequence in sense or antisense orientation in gene therapy are also protected.
CN102920692A Application of (E)-2-(1-hydroyxl-4-cyclohexanone) aethyl-caffeic acid phenethyl ester in preparation of medicament for preventing and treating rheumatoid arthritis The invention provides application of (E)-2-(1-hydroyxl-4-cyclohexanone) aethyl-caffeic acid phenethyl ester in the preparation of a medicament for preventing and treating rheumatoid arthritis. The structural formula of the (E)-2-(1-hydroyxl-4-cyclohexanone) aethyl-caffeic acid phenethyl ester is shown as the specification. The (E)-2-(1-hydroyxl-4-cyclohexanone) aethyl-caffeic acid phenethyl ester is used in animal pharmacodynamic tests, and results indicate that the (E)-2-(1-hydroyxl-4-cyclohexanone) aethyl-caffeic acid phenethyl ester can remarkably inhibit the attack degree and attack rate of CIA (collagen-induced arthritis), can reduce the LTB4 (leukotrienes B4) level of CIA mouse plasma and joints, lower the expression index of mRNA (messenger ribonucleic acid) and protein of 5-lipoxygenase of joints, reduce aggregation of joint inflammatory cells and damage of synovial membrane, and can particularly protect bone injury. Therefore, the (E)-2-(1-hydroyxl-4-cyclohexanone) aethyl-caffeic acid phenethyl ester can be used for preparing a medicament for treating rheumatoid arthritis. The medicament is a medicinal composition prepared from the (E)-2-(1-hydroyxl-4-cyclohexanone) aethyl-caffeic acid phenethyl ester serving as an active component and conventional drugs as carrier. The medicament comprises tablets, dispersible tablets, lozenge, orally disintegrating tablets, sustained-release tablets, capsules, soft capsules, dropping pills, granules, injection, powder-injection or aerosol and the like. The medicament has great clinical application value.
US20120094978 Ocular Allergy Treatments Compositions, kits and methods for the treatment or prevention of ocular allergies and inflammation and the symptoms thereof comprising alcaftadine or a pharmaceutically acceptable salt thereof.
WO2009113512A1 Socs3 expression promoter, drug and food containing the same and method of promoting the expression of socs3 An SOCS3 expression promoter which contains hyaluronic acid having an average molecular weight of 500,000 or more and/or a salt thereof as the active ingredient.
US20070134183 Aminosulfonic acid compounds for promoting desquamation of the skin Aminosulfonic acid compounds having the structural formula (I): are suited for promoting desquamation of the skin and/or stimulating epidermal renewal and/or combating aging of the skin.
WO2011154580A1 Novel cxcr4 inhibitors as anti-hiv agents The invention relates to compounds having formula (I), and the pharmaceutically acceptable salts and hydrates and solvates of same, and to the use thereof as anti-HIV agents in the treatment of Acquired Immune Deficiency Syndrome (AIDS). The invention also relates to a method for obtaining same, to the synthesis intermediates used in said method, and to a method for the treatment of AIDS by means of the administration of said compounds.
CN101041069A Preparation for beauty and for supplementing blood The invention relates to a composite agent, which uses collagen (or polypeptide) and boletic acid ferrous iron (or iron compound) as material to be mixed and processed. The invention can feed collagen and iron element to realize beauty treatment, with simple process, low cost, and wide application.
CN103127073A Application of Eryngiolide A in anti-platelet aggregation medicines The invention relates to application of Eryngiolide A in preparation of anti-platelet aggregation medicines. Use of the Eryngiolide A in preparation of anti-platelet aggregation medicines is made public for the first time, the skeleton type is completely novel, and the Eryngiolide A has an unexpectedly high anti-platelet aggregation inhibitory activity, probability of other compounds giving any revelation for the Eryngiolide A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in anti-platelet aggregation.
WO2012173952A1 Piperazine derivatives, compositions, and uses related thereto The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.
US8268785 Use of a Pde 5 inhibitor for treating and preventing hypopigmentary disorders The invention relates to the use of PDE5 inhibitors, preferably sildenafil or tadalafil, optionally in combination with a further active ingredient, for treating and/or preventing hypopigmentary disorders.
CN101024089A Function of E4BP4 gene inplantation course and use thereof The present invention discloses a new application of E4BP4 gene, it can be used as regulator for regulating embryo nidation (embryo implantation). In prophase of embryo nidation it can block expression of E4BP4 gene or close the biological function of its expression product E4BP4 protein, so that it can inhibit embryo nidation, otherwise it can promote nidation; in anaphase of embryo nidation it can block expression of E4BP4 gene or close the biological function of its expression product E4BP4 protein, so that it can promote embryo nidation, otherwise, it can inhibit nidation.
WO2005023236A1 Phenylephrine tannate, pyrilamine tannate, and dextromethorphan tannate salts in pharmaceutical compositions Compositions of tannate salts of phenylephrine, pyrilamine, and dextromethorphan produced by a method that allows for the in-situ conversion and incorporation of the tannate salts in a single dosage form. The conversion process includes dissolving salts of phenylephrine, pyrilamine, and dextromethorphan in a solvent and mixing with a dispersing agent and tannic acid to generate tannate salts. The tannate salts may be further processed without further purification or isolation to single dosage forms, such as tablets and suspension.
WO2013139423A1 Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with other anti-tumor compounds A pharmaceutical composition of 3-(1-{3-[5-(1-Methyl-piperidin-4-ylmethoxy) pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile or a pharmaceutically acceptable salt and/or solvate thereof in combination with compound selected from the group erlotinib, cetuximab, aflibercept, bevacizumab.
US20100331237 Gag binding proteins A method is provided for introducing a GAG binding site into a protein comprising the steps: identifying a region in a protein which is not essential for structure maintenance introducing at least one basic amino acid into said site and/or deleting at least one bulky and/or acidic amino acid in said site, whereby said GAG binding site has a GAG binding affinity of Kd≦10 μM, preferably ≦1 μM, still preferred ≦0.1 μM, as well as modified GAG binding proteins.
EP1513803B1 Ligands that are inhibitors of the rar receptors Novel ligands that are inhibitors of the RAR receptors, process for preparing them and use thereof in human medicine and in cosmetics. The invention relates to novel bicyclic compounds corresponding to the general formula (I) and to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine, or alternatively in cosmetic compositions.
US20080176897 Substituted Quinolone Carboxylic Acids, Their Derivatives, Site of Action, And Uses Thereof Substituted quinolone carboxylic acids and their derivatives are described. These compounds modulate the effect of γ-aminobutyric acid (GABA) via a novel site on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.
EP1756082A1 5-morpholinylmethylthiophenyl pharmaceutial compounds as p38 map kinase modulators The invention provides compounds of the formula (I) or a salt, solvate or N-oxide thereof, wherein:R1 and R2 are the same or different and each is selected from hydrogen, saturated C1-3 hydrocarbyl, halogen and cyano; X is selected from C=O, C=S, C(=O)NH, C(=S)NH, C(=O)O, C(=O)S, C(=S)O and C(=S)S; R3 is selected from aryl and heteroaryl groups each having from 5 t0 12 ring members and being unsubstituted or substituted by one or more substituent groups R10 as defined in the claims; R4 and R5 are the same or different and are selected from hydrogen and methyl; or one of R4 and R5 is selected from hydroxymethyl and ethyl and the other is hydrogen; and R6 and R7 are the same or different and are selected from hydrogen and methyl. The compounds of the formula (I) hayed activity as p38 MAP kinase and Taf kinase inhibitors.
WO2011047315A1 Subsitituted benzimidazoles This invention relates to novel substituted benzimidazoles and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound that modulates theGABAA receptor. This invention also provides novel intermediates for the preparation of the compounds of the invention, and salts thereof.
CN1850071A Bifendate solid dispersible, and its preparing method and low-release preparation containing same The present invention relates to the field of medicine preparation. In the concrete, it relates to a biphenyldiester solid dispersion and its delayed release preparation containing said biphenydiester solid dispersion. Besides, said invention also discloses its preparation method. Said invention can raise bioavailability of medicine, can retain effective blood concentration for 12 hr.
CN1628652A Method for treating palmar fascia and plantar aponeurosis fibromatosis The invention discloses a method for treating palmar fascia and plantar aponeurosis fibromatosis which comprises, applying the patients by therapeutic active agent of composition containing 13-cis retinoic acid, preferably, the methods of treatment comprises applying the patients by initial dose of composition containing 13-cis retinoic acid at the preliminary therapeutic period, then applying the composition of maintenance dose.
WO2005016331A1 Therapeutic agent for neuropathic pain containing n-(benzoyl)amino acid derivative as active ingredient [MEANS FOR SOLVING PROBLEMS] A preventive and/or therapeutic agent for neuropathic pains, characterized by containing a compound represented by the following formula (I), an optically active isomer thereof, or a pharmaceutically acceptable salt of either as an active ingredient. (Chemical formula 1) (I) (In the formula, Z is -C(CH3)2- or -CH(CH(CH3)2)-; n is 0 to 2; R1 represents C1-4 alkyl, hydroxy, trifluoromethyl, or acetoxy; and R2 represents hydrogen or C1-4 alkyl, provided that the case where Z is -CH(CH(CH3)2)- and R1 is 2-position hydroxy is excluded.) [EFFECTS] The agent is capable of oral administration, is reduced in side effects, and is safer. It is highly effective in the prevention of and/or treatments for neuropathic pains and is pharmaceutically excellent.
WO2009031879A1 Pharmaceutical composition combining betamethasone (steroidal anti-inflammatory agent) and methocarbamol (muscle relaxant) and use thereof in the treatment of musculoskeletal diseases The invention relates to a pharmaceutical composition comprising the synergic combination of a steroidal anti-inflammatory agent, such as the active principle betamethasone in the form of the pharmaceutically acceptable phosphate and dipropionate salts thereof, and a centrally acting muscle relaxant, such as the active principle methocarbamol, as well as pharmaceutically acceptable excipients, which are formulated in a single dosage unit intended for intramuscular administration. The composition, which is used to control and treat inflammatory musculoskeletal diseases accompanied by muscle contracture, provides improved therapeutic effect, faster action in less time and a reduction in the risk of side effects, such as drowsiness and inability to perform daily tasks.
CN102600075A Danofloxacin mesylate suspension and preparation method thereof The invention discloses a danofloxacin mesylate suspension and a preparation method thereof. The danofloxacin mesylate suspension comprises the components of danofloxacin mesylate powder, aluminum monostearatre serving as a suspending agent, phosphatidylcholine serving as a dispersing agent, tween-80 serving as a wetting and emulsifying agent, 2,6-butylated hydroxytoluene and butylated hydroxyanisole serving as antioxidants. The invention also provides a preparation method of the suspension, which comprises the steps of: dissolving the aluminum monostearatre in oil, screening, adding the phosphatidylcholine, the tween-80, the 2,6-butylated hydroxytoluene and the butylated hydroxyanisole serving as the antioxidants, then placing in a dispersing machine for dispersing, then transferring to a colloid mill for circulating, and taking out to obtain the danofloxacin mesylate suspension. The danofloxacin mesylate suspension is a faint yellow and slightly-thick suspension. According to the danofloxacin mesylate suspension provided by the invention, effective components of medicines can be slowly released, bioavailability of the medicines can be improved, treatment effects of the medicines can be enhanced, and effective blood concentration time can maintain above 60h after once medication. The danofloxacin mesylate suspension is low in cost because no special solvent is needed during production, is simple in production process, and is easy to industrialize.
WO2014126370A1 Film-forming pharmaceutical composition for wound healing and method for preparing the same The present invention relates to a pharmaceutical composition for forming a film directly on a wound to accelerate wound healing, a use for the same, a treatment method using the same, and a method for preparing the same. The film-forming composition according to the present invention forms a film directly on the wound to increase the adhesion to the wound. The formed thin hydrophilic film protects the wound surface to prevent infection of the wound surface, retains the physiologically active substance useful for wound healing on the wound surface to promote the wound healing, and allow drugs to be continuously delivered to the wound surface. Therefore, the composition according to the present invention has excellent wound healing effect and has excellent usability as it is not absorbed into clothing, bandage, etc., thus effectively replacing conventional gel or ointment formations for delivering physiologically active substances.
WO2010118010A1 Combination of decitabine with cytidine deaminase inhibitor and use thereof in the treatment of cancer Provided herein are methods of treating cancer comprising administering decitabine in combination with compounds that inhibit the deamination enzyme responsible for the inactivation of decitabine.
CN103284992A Application of Phomopsone C for preparing antiviral medicine The invention discloses a novel application of a Phomopsone C compound for preparing an antiviral medicine. Thus, the novel application of Phomopsone C is developed.
US7259170 Macrolides containing pharmaceutical compositions A pharmaceutical compound comprising a compound of formula I and a pharmaceutically acceptable 2-amino-1,3-propanediol beside one or more pharmaceutically acceptable excipient(s).
CN101044902B Health-care product for reducing weight and lowering cholesterin content in blood A health-care food for reducing weight and decreasing cholesterol is prepared from the refined conjak starch through purifying to obtain high-purity glucomannan, and linking a certain number of polyarginines or polylysines to its hydroxy group.
US20130101666 Liposome including elastin-like polypeptide conjugated to moiety containing hydrophobic group, chemosensitizer and anticancer agent and use thereof A liposome including a lipid bilayer, an elastin-like polypeptide (ELP) conjugated to a hydrophobic moiety; a chemosensitizer; and an anticancer agent, a pharmaceutical composition including the same, and a method of delivering a chemosensitizer and an anticancer agent to a target site of a subject by using the liposome.
EP1791599A1 Combination of a 5-ht(1) receptor agonist and an alpha-2-delta ligand for the treatment of migraine The present invention relates to a combination of 5-HT1B, 5-HT1D or 5-HT1F agonist and an alpha-2-delta ligand. Such a combination is useful in the treatment of pain, particularly the pain arising from migraine.
EP2129373A1 Novel use of genistein Use of genistein for the treatment and prevention of dry eye syndrome or LKC and corresponding compositions containing it.
US20070269393 Topical anesthetic formulation The topical medicament gel formulation of the present invention includes an anesthetic, an anti-microbial, an oxidant, a nutrient, a diuretic, an opioid, an anti-emetic, an anti-seizure drug, and a non-steroidal anti-inflammatory drug (NSAID), USP in a molecular, as opposed to a salt form, as the active ingredient. Additional constituents illustratively include a skin penetration enhancer and a gelling agent. This invention deals with problems commonly associated with topical application of local medicaments such as: slow onset of action; need for occlusion; and rapid loss of effect due to rapid systemic dispersion. The invention permits enhanced penetration of the medicament and thereby allows for a lesser total dosage of pharmaceutically active ingredient. The use of a lesser total dosage also decreases systemic toxicity.
CN103421021A Compound divorced from gamboge resin, derivative of compound, and pharmaceutical composition containing compound and derivative The invention provides a compound divorced from gamboge resin, a derivative of the compound, and a pharmaceutical composition containing the compound and the derivative. The chemical formula (I) of the novel compound is shown in the description, wherein the definition for every substituent is shown in the description and patent claim. The invention also discloses an acetone extraction product of the compound and the gamboge resin, and an application of a divorcing part of the acetone extraction product in preparing pharmaceutical composition.
CN1859917A Medicine and food/beverage for ameliorating hyperglycemia A compound having a cyclolanostane framework, e.g., 9,19-cyclolanostan-3-ol or 24-methylene-9,19-cyclolanostan-3-ol, is used as an active ingredient for a medicine or a food/beverage for ameliorating hyperglycemia.
US20080299089 Endogeneous repair factor production promoters It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) 12 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.
CA2321122C E-2-[4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy]ethanol and pharmaceutical compositions thereof The present invention relates to E-2-[4(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy]ethanol useful in lowering serum cholesterol and to pharmaceutical compositions thereof. A method of lowering serum cholesterol and a method for the prevention or treatment of atherosclerosis is also disclosed.
WO2007116052A1 Oral composition comprising dha and genistein for enhancing skin properties Composition for oral consumption in the form of a substantially 5 homogeneous aqueous emulsion, suspension or dispersion comprising genistein and docosahexaenoic acid (DHA) and less than 1% by weight of soy protein, wherein the weight ratio of genistein to DHA is in the range of from 1:100 to 1:1, the composition comprises genistein in an amount of from 0.0001% to 0.1% by 10 weight and the genistein and DHA exhibit an anti-ageing effect on skin.
CN101904856A Application of 1,6-diphosphofructose and derivative thereof in preparing animal medical health care products The invention relates to an application of 1,6-diphosphofructose and a derivative thereof in preparing animal medical health care products, belonging to the field of health care products for animals. The 1,6-diphosphofructose and the derivative thereof are applied to preparing medicines for preventing or curing myocardial ischemia, angiocardiopathy, shock and various untoward effects caused by energy shortage and enhancing the immunity of the animals. Every kilogram of the animals need 250-1,000 mg of the 1,6-diphosphofructose or the derivative thereof per 1kg of weight every day, and the 1,6-diphosphofructose or the derivant thereof is used once a day for 3-5 consecutive days. The invention provides a new application range for energy reinforcers of the 1,6-diphosphofructose and the derivative thereof which are widely used for national clinic on human, provides new resources for the research field of veterinary medicines and also provides excellent animal medical health care medicines for livestock breeding.
CN102002053A Tetrahydro thienopyridine derivative for treating The invention provides a novel tetrahydro thienopyridine derivative. The dosage of one or more active compounds in the novel tetrahydro thienopyridine derivative is 0.1-20mg/kg body weight, and the preferable dosage is 0.1-5mg/kg body weight. The novel tetrahydro thienopyridine derivative can be used for producing medicines for preventing and/or treating diseases induced by thrombosis or thromboembolism.
EP2588092A1 Use of squaramide in the prevention and/or treatment of rosacea A compound of formula (I): or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, or hydrate thereof are described. Also described, is the use of such a compound, salt, solvate or hydrate in the preparation of a medicament intended to treat rosacea.
US20080119548 Control Of Feeding Behavior By Changing Neuronal Energy Balance Obesity is a worldwide health issue, affecting children and adults in developed and developing countries. Obesity is a disorder of both energy metabolism and appetite regulation, and may be understood as a dysfunction of energy balance. Applicants have found a means for regulating food intake by a subject by administering a compound to the subject which affects neuronal energy balance. Applicants have found a means for regulating food intake by a subject administering a compound to the subject which targets the activity of AMPK, in particular inhibiting activation, in particular hypothalamic. Applicants have also found a method of inducing weight loss in a subject by decreasing the subjects appetite by administering a compound to the subject which increases the subject's neuronal energy balance.
CN101259279A Biocompatibile monodisperse nano polymer carrier and its preparation and medicine-carrying method The invention relates to a monodisperse nano-polymer carrier with biological compatibility and a method for preparation and carrying drug thereof. Firstly, a reversible addition fragmentation chain transfer (RAFT) polymerization method is used for preparing amphiphilic block copolymers with smaller polydispersity index, wherein the hydrophilic segment is methylacryoyloxyethyl phosphorylcholine (MPC) and the hydrophobic segment is n-butyl methacrylate (BMA). Then through the method of solvent evaporation, the amphiphilic block copolymers are used for preparing nano-polymer micelle, drugs are encapsulated in the micelle through physical action, thus obtaining the monodisperse nano-polymer carrier system with good biological compatibility.
CN1778823A Homogeneous tremella polysaccharide modifier with multiple biological activity, its production and preparation containing them A homogeneous tremella polysaccharide with multiple biological activity modifier, its production and preparation containing them are disclosed. The process is carried out by taking out homogeneous polysaccharide TF, adding into anhydrous formamide, adding into esterification agent at 30-80íÒC, agitating, laying aside at room temperature for 1 day, neutralizing pH to 6-7 by NaOH, filtering, dialyzing the filtrate by distilled water and precipitating out deposit by alcohol to obtain compound STF.
CA2449066C Nicotine-containing film preparation A film preparation of a three-layer structure which comprises: a nicotine-containing layer having a 180~ peel strength in application to a Bakelite plate of 1 to 30 g/20 mm and a solubility in water of 3 to 10 minutes and comprising nicotine and an edible water-soluble polymer; and two coating layers superposed respectively on both sides of the nicotine-containing layer, the coating layers each having a 180~ peel strength in application to a Bakelite plate of 100 to 500 g/20 mm and a solubility in water of 0.5 to 3 minutes and comprising a water-soluble and non-water-absorbing polysaccharide and/or an edible polymer and a softener.
US20060134668 Methods for treating patients and identifying therapeutics The disclosure provides, among other things, molecular markers for categorizing the neoplastic state of a patient and methods for using the molecular markers in designing, screening and targeting therapeutic agents for the treatment of colon cancer.
US20120009216 Early detection of flaviviruses using the ns1 glycoprotein The invention concerns a method for early detection of a flavivirus-induced infection, comprising the detection of the flavivirus non-structural glycoprotein NS1 in a biological sample during the clinical phase of the infection, by an immunological method using at least two identical or different antibodies, the first antibody consisting of polyclonal or monoclonal antibodies pre-selected for their high affinity for said NS1 protein hexameric in shape.
US20120302633 Novel polymorph of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphthalenyl) ester Herein described is a novel crystalline form of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphtalenyl) ester. In particular, herein described is a polymorph of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphtalenyl) ester, characterized by a Powder X Ray Diffraction spectrum as indicated in FIG. 1, and/or by a DSC profile as indicated in FIG. 2, and/or by a TGA profile as indicated in FIG. 3 and/or by an IR spectrum as indicated in FIG. 4.
CN101172975B Method of preparing five-alkaloid composition of corydalis saxicola bunting The invention relates to a preparation method for corydalis saxicola bunting five-alkaloid compound. The method comprises the steps as follow: (1) one proportion of corydalis saxicola bunting total alkaloid crude extract is prepared and back-flew and dissolved through 10 to 100 parts (V/W) of ethanol solution with concentration of 75 to 100 percent, and 0.5 to 5 parts (W/W) of silica gel mixed sample is added into the solution, and the solution is then mixed and steamed out so as to obtain mixed sample silica gel; (2) 6 to 20 parts (W/W) of silica gel are dipped in 5:1 to 1:1 (V/V) of ethyl acetate and ethanol, and then are poured into a column in a wet way, and the mixed sample silica gel obtained from step (1) is added in, and then is processed through gradient elution with 3:1 to 1:1 (V/V) of ethyl acetate and ethanol; part of 1/1 elution liquid is collected, and then the filtered residues are collected after condensing and filtering the liquid; and the corydalis saxicola bunting five-alkaloid compound is obtained by drying the filter residues. The invention has the advantages of simple device, low cost, easy operation, short time taken, high yield and high safety.
EP1158978B1 Medicament against dysmenorrhoea and premenstrual syndrome comprising lidocaine A local anesthetic is used for the manufacture of a medicament for use against dysmenorrhoea and premenstrual syndrome and for increasing fertility. A pharmaceutical composition may also be used that comprises a pharmaceutically effective dose of a local anesthetic together with a pharmaceutically acceptable excipient. The invention also relates to a process for reducing dysmenorrhoea and premenstrual syndrome symptoms in a woman with said pharmaceutical composition. The pharmaceutical composition may be administered by pertubation.
US20060154969 Adenosine receptor selective modulators The invention relates to the compounds of formula (I), to a method for producing the same and to the use thereof as medicaments.
US20130029957 17-Hydroxyprogesterone Ester-Containing Oral Compositions and Related Methods The present invention provides for bioavailable oral dosage forms containing esters of 17-hydroxyprogesterone as well as related methods. The oral dosage forms can be formulated for pregnancy support and can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. In another embodiment, a pharmaceutically acceptable oral dosage form for pregnancy support is provided. The pharmaceutically acceptable oral dosage can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. The oral dosage form can, when measured using a USP Type-II dissolution apparatus in 900 mL of deionized water with 0.5 (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., release at least 20 wt % of the dose of the ester of 17-hydroxyprogesterone after 60 minutes, or in the alternative release at least 20 wt % more after 60 minutes than an equivalently dosed oral dosage form without the carrier.
CN101926805A Pharmaceutical composition containing 16, 17 isoxazolidine steroidal compound The invention relates to a pharmaceutical composition containing a 16, 17 isoxazolidine steroidal compound, which is characterized by containing a compound (I) as an active ingredient and one or more pharmaceutically acceptable excipients which are applicable to oral administration, and R1 is selected from C1-C4 alkyl and C3-C6 cycloalkyl. R2 is selected from H or C2-C4 alkyl carbonyl, and the content of the compound (I) is equivalent to the daily dose of 2-1000 mu g/kg.
US20070254044 Antimicrobial Amorphous Compositions The present invention comprises compositions and methods for providing antimicrobial compositions. The antimicrobial compositions comprise gel delivery vehicles comprising stabilized silver, wherein ionic silver is provided to a site for antimicrobial purposes. Methods of making and using such compositions are taught, including application of the silver-containing gel compositions to wounds, burns, abrasions, cuts, surgical incision, sites where skin or organ integrity has been breached, and other sites to supply an antimicrobial environment.
WO2014042433A3 Compounds and compositions for modulating adenosine a3 receptor activity The present invention provides for Adenosine A3 receptor agonists, and also methods and use of the compounds of the invention, by themselves or in combination with other therapies, for treating a disease, disorder, or condition.
CN101099749A Composition containing lactobacillus acidophilus and bidifobacterium longum and application thereof The present invention relates to a composite containing acidphilous lactobacillus LA-Onlly CGMCC No.2106 and long-bifidobacterium BL88-Onlly CGMCC No.2107 and its application. Besides, said composite also contains oligosaccharide and vitamins, so that said composite can be used as food, medicine and health-care product. It is mainly used for regulating enteric microbial pool and raising immunity.
CA2554859A1 A process for preparing an injectable sterile pharmaceutical formulation containing at least piperacillin sodium and tazobactam sodium active principles Mixtures of at least two active principles, of which at least one is the sodium salt, are precipitated from an organic solution containing the same active principles in salified or non-salified acid form.
EP1062209B1 Metabolically inert anti-inflammatory and anti-tumor antifolates Hether to unknown metabolically inert classical folate analog inhibitors of the enzyme Dihydrofolate Reductase [DHFR] that are transported to tumor cells via the reduced folate receptors are provided. These compounds exhibit superior anti-asthmatic responses in rabbits relative to methotrexate and the standard drug theophylline. The title compound 4-amino-4-deoxy-5,8,10-trideaza-pteroyl-4'-methyleneglutamic acid (1) exhibited outstanding anti-tumor activity. Compound (1) was 1,000 to 10,000 times more active than methotrexate in causing total growth inhibition (TGI) of a number of human tumor cells in culture. Unlike methotrexate the TGI values of (1) are in the range of therapeutically relevant concentrations. Tumor cells that are resistant to methotrexate by virtue of defective polyglutamylation were 3-4 times more collaterally sensitive to compound (1). (1) was completely inert on incubation with folylpolyglutamate synthetase. On treatment of (1) with a preparation of aldehyde oxidase no oxidative activity was uncovered. Compound 1 was totally resistant to hydrolytic cleavage of the glutamate moiety by carboxypeptidase derived from Pseudononad sp. These biochemical and pharmacological properties of the metabolically inert classical antifolates establish their clinical utility and superiority as new and novel anti-inflammatory and anti-tumor agents exhibiting enhanced target enzyme specificity and lower toxicity.
WO2005030733A1 Benzimidazole derivatives, compositions containing them, preparation therof and uses thereof Compounds of Formulae (IA), (IB) or pharmaceutically acceptable salts thereof; wherein Het, X1, R1, R2, R3, R3a and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
DE102004046583A1 New D-xylopyranosyl-phenyl-substituted cycle compounds useful for treating e.g. diabetes mellitus, complications of diabetes, metabolic acidosis or ketosis D-xylopyranosyl-phenyl-substituted cycle compounds, their tautomers, stereoisomers, mixtures and salts are new. D-xylopyranosyl-phenyl-substituted cycle compounds of formula (I), their tautomers, stereoisomers, mixtures and salts are new. X = e.g. H, 1-6C alkyl, 2-6C alkynyl, 2-6C alkenyl, 3-10C cycloalkyl, 5-10C cycloalkenyl, (hetero)aryl, arylcarbonyl, piperidin-1-ylcarbonyl, bromomethyl, iodomethyl or cyano (the alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl groups are optionally partly or totally fluorinated or mono- or disubstituted by chlorine, cyano, hydroxy, mercapto, 1-3C alkoxy or 1-3C alkyl, and in cycloalkyl and cycloalkenyl groups, one or two methylene groups are optionally replaced by O, S, CO, SO or SO2 and in N-heterocycloalkyl groups a methylene group is optionally replaced by CO or SO2); (MK#2) Cy = a 5- or 6-membered saturated or monounsaturated carbocyclic ring, optionally comprising 1 - 3 heteratoms of N, O and S, and is substituted by R4-R6 through a single bond and by R3 through a single or double bond, and one or two methylene groups are optionally replaced by CO or a sulfanyl group SO or SO2 and at least one H atom bound to carbon is optionally replaced by fluorine); Z = -O-, -CH2-, -CH=, -NRn-, -S-, -SO- or -SO2- (H atoms of the methylene or methanylylidene bridge is optionally substituted by CH3 or F); R1 = e.g. H, halogen, 1-6C alkyl, 2-6C alkynyl, 2-6C alkenyl, 3-10C cycloalkyl, 1-6C alkyloxy (the (cyclo)alkyl, (cyclo)alkenyl or alkynyl are partly or totally fluorinated or mono- or disubstituted by chlorine, hydroxy, 1-3C alkoxy or 1-3C alkyl, and in cycloalkyl and cycloalkenyl groups, 1 or 2 methylene groups are optionally replaced by O, S, CO, SO or SO2, and in N-heterocycloalkyl groups, a methylene group is optionally replaced by CO or SO2); R3 = e.g. H, halogen, 1-6C alkyl, 2-6C alkynyl, 2-6C alkenyl, 3-10C cycloalkyl, (hetero)aryl; R4 = e.g. H, F, Cl, cyano, nitro, amino, 1-3C alkyl-amino, di-(1-3C alkyl)amino, 1-3C alkylcarbonylamino, 1-3C alkyl, 1-3C alkoxy, hydroxycarbonyl, 1-3C alkoxycarbonyl or methyl or methoxy (mono-trisubstituted by fluorine atoms); R5 = e.g. H, F, Cl, cyano, 1-3C alkyl, 1-3C alkoxy or methyl or methoxy (mono--trisubstituted by fluorine atoms); R4+R5 = 1-4C alkylene or 2-4C alkenylene bridge which forms an anellated or bridged bicyclic group with 2-4 atoms of the Cy ring and optionally partly or wholly fluorinated or mono- or disubstituted by chlorine, hydroxy, 1-3C alkoxy or 1-3C alkyl, and 1 or 2 methylene groups are optionally replaced by O, S, CO, SO, SO2 or NRn; R6 = H, 1-3C alkyl or fluorine; R4+R5+R6 = 3-6C alkanetriyl bridge, which together with the Cy ring forms a bridged bicyclic or a tricyclic system (the alkanetriyl bridge is optionally mono or polyfluorinated or mono or disubstituted by chlorine, hydroxy, 1-3C alkoxy or 1-3C alkyl, and 1 or 2 methylene groups are optionally replaced by O, CO, SO2 or NRn); E = e.g. oxygen, (fluoro)methylidene, chloromethylidene, 1-6C alkylmethylidene; Rn = H or 1-4C alkyl; R7a-R7c = H, (1-18C alkyl)carbonyl, (1-18C alkyl)oxycarbonyl, arylcarbonyl or aryl-(1-3C alkyl)-carbonyl. The dotted line represents a single or double bond. Provided that X excludes hydroxymethyl. [Image] - ACTIVITY : Vasotropic; Antidiabetic; Antilipemic; Antiarteriosclerotic; Anorectic; Hypotensive; Cardiant; Anti-inflammatory; Ophthalmological; Nephrotropic; Neuroprotective; Antiulcer. - MECHANISM OF ACTION : Inhibitors of sodium-dependent glucose cotransporter SGLT (particularly SGLT2 and SGLT1).
WO2011133210A3 A method treating breast cancer The present invention relates, in general, to breast cancer and, in particular, to methods of treating breast cancer comprising administering to a subject in need thereof an agent that modulates signal transduction regulated by β-arrestin (e.g., β-arrestin 1). The invention further relates to methods of identifying compounds suitable for use in such methods.
EP2680826A1 Vitamin d composition The present disclosure relates to high dosage vitamin D formulations, in particular vitamin D3 that can be used for the treatment of vitamin D deficiency and insufficiency.
WO2010150206A1 N-substituted-n-phenylethylsulfonamides for the identification of biological and pharmacological activity Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides of formula (I) useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
US20070249051 Vinyl-phenyl derivatives for inflammation and immune-related uses The invention relates to compounds of structural formula (Ia): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, X4, X6, X10, R1, Y, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
US20080255193 Comprising NK3 receptor antagonist talnetant, povidone, erythritol and Sodium Lauryl Sulfate; erythritol used as soluble filler in preparation of stable drug; dosage tablet or capsule A novel pharmaceutical composition comprising the NK3 receptor antagonist talnetant, povidone, mannitol and a surfactant, and a process for its preparation are disclosed.
EP1720552A2 Methods for treating inflammatory and autoimmune diseases The present invention provides methods for treating inflammatory conditions, rheumatoid diseases, autoimmune conditions, and conditions associated with bone loss, comprising administering to a subject with an inflammatory condition an amount effective to treat the condition of a compound selected from the group consisting of narcistatin, pancratistatin, pancratistatin-7' phosphate and pancratistatin-3',4' cyclic phosphate, or pharmaceutically acceptable salts thereof.
WO2006094843A1 Piperazine derivatives as glyt1 inhibitors The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
EP2197886A1 5-cyano-thienopyridines for the treatment of tumors The invention relates to novel 5-cyano-thienopyridines of the formula (I) where R1, R2, and R3 have the meanings designated in Claim 1. Said 5-cyano-thienopyridines are inhibitors of TGF beta receptor kinase and may be used, among other things, for the treatment of tumors.
WO2006014653A1 Induction of apoptosis in toll-like receptor expressing tumor cells Some types of cancer cells express one or more Toll-like receptors (TLRs). These TLRs are therapeutic targets. The invention relates to methods for treating Toll-like receptor expressing cancers and tumor cells by selecting a TLR expressing tumor cell and contacting the cell with a therapeutically effective amount of a TLR ligand. The invention particularly relates to methods for treating TLR3 expressing cancers and tumor cells using TLR3 agonists.
CN101897701B Preparation method of amoxicillin and clavulanate potassium tablets The invention discloses a preparation method of amoxicillin and clavulanate potassium tablets, comprising the following steps: (a) weighing the following main and auxiliary materials: 120-135 parts of amoxicillin, 40-45 parts of clavulanate potassium, 27-32 parts of microcrystalline cellulose, 1-3 parts of croscarmellose sodium (ADS), 1-3 parts of superfine silica powder and 2-4 parts of magnesium stearate; (b) after pelletizing amoxicillin, mixing the pelletized amoxicillin with clavulanate potassium according to the mass ratio of 4:1 to form the main materials; (c) uniformly mixing the auxiliary materials including superfine silica powder, ADS and microcrystalline cellulose by the method of increment by equal quantity and throwing the main materials and the auxiliary materials into a mixer by the method of increment by equal quantity to be mixed for 36-70min; and (d) tabletting the mixed powder. The products prepared by the method have bright, clean and beautiful appearances and stable content and dissolution.
CN103191404A Medicine for treating nose bleeding and preparation method thereof The invention discloses a medicine for treating nose bleeding and a preparation method thereof. The formula of the medicine comprises the following components by weight percent: 30% of animal protein extract, 30% of fresh white pomegranate petal, 15% of western medicine antibiotics and 25% of pearl powder. The preparation method of the medicine for treating nose bleeding comprises the following steps: a, washing the animal protein extract, drying, crushing, filtering (protein of poultry eggs with egg shells and egg yolks removed can be treated from the step), absorbing by resin, eluting, standing for deposition for 8-12 hours, concentrating, freezing and drying; b, washing fresh pomegranate petal, drying, baking in an oven at 60 DEG C and then crushing; and c, evenly mixing 30% of the treated animal protein extract, 30% of the treated fresh white pomegranate petal, 15% of western medicine antibiotics and 25% of pearl powder. The medicine for treating nose bleeding is suitable for persons at all ages, and has no toxic or side effect.
WO2007019346A1 Benzothiazoles and thiazolopyridines as sirtuin modulators Provided herein are benzothiazol and thizolopyridine derivatires which are sirtuin-modulating compounds and methods of use thereof . The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/ or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent .
US8067425 Neuroprotective bicyclic compounds and methods for their use Embodiments of this invention provide novel cyclic compounds structurally related to diketopiperazines and methods for their therapeutic use. Such compounds are neuroprotective and have utility as therapeutic agents for treatment of diseases, injuries and other conditions characterized by neuronal degeneration and/or death. Compounds are also useful for manufacture of medicaments useful for treatment of such conditions.
CN101530388A Formulation of mildronate injection and preparation method The invention relates to a formulation of mildronate injection and a preparation method. The formulation mainly comprises active component of mildronate, phosphate buffer solution, and water for injection. The preparation method for the formulation comprises the following steps: weighing each component, stirring and decomposing the components, adding 0.05 percent of active carbon in weight-volume ratio into the components, pressurizing and filtering liquid medicine to remove pyrogen, adjusting the pH value of the solution within a range of 7.0 to 8.5, preliminarily filtering the solution by using a filter membrane of 0.45mu m, then fine filtering the solution by using a filter membrane of 0.22mu m, filling the solution into a penicillin bottle of 5 milliliters after passing quality inspection, and capping and sealing the bottle; and finally a temperature of 121 DEG C, sterilizing the bottle for 20 minutes under terminal sterilizing condition to obtain the injection. The mildronate injection produced by the method has high sterility assurance degree, each index accords with the prescription after being stored for three years, and the safety is fully ensured for clinical application.
WO2012115575A1 Derivatives for inducing osteogenic differentiation The present invention relates to a compound for use as a medicament, especially for treating bone, tooth and cartilage related diseases and damages. The compound has shown to be inducing and enhancing osteogenic differentiation. The present invention further relates to implants comprising said compound.
US20120148633 Binary and tertiary galvanic particulates and methods of manufacturing and use thereof The present invention relates to galvanic particulates, their methods of manufacture and uses in treatments are described. The galvanic particulates may be binary or tertiary galvanic particulates, for example, containing multiple layers or phases of conductive materials.
WO2006098519A1 Pyrazolopyrimidine derivative or pharmaceutically acceptable salt thereof A pyrazolopyrimidine derivative represented by the general formula (I) and a pharmaceutically acceptable salt thereof exhibits excellent MAPKAP-K2 inhibitory activity. A pharmaceutical agent comprising the compound as the active ingredient is expected to be useful for the treatment of MAPKAP-K2-mediated disorders including inflammatory disorders, autoimmune disease, destructive bone disorders, cancer and/or tumor growth.
WO2012050589A1 Methods for treating hyperuricemia and related diseases Provided herein are methods of treating gout, treating hyperuricemia, lowering serum uric acid, or the like with compounds of formula (I) have the following structure Further, provided herein are compositions comprising a compound of formula (I).
CN101327187A Nonoxynol nonylphenoxy-polyethoxyethanol suppositorium and preparation method thereof The invention discloses a novel nonoxynol-9 suppository and a preparation method thereof, and the nonoxynol-9 suppository is composed of the raw materials with the following weight portions of 1 portion of nonoxynol-9, 2 portions of polyethyleneglycol 1000 and 13 portions of mixed fatty glyceride. The nonoxynol-9 suppository of the invention optimally selects new stroma which replaces the traditional stroma adopted in the nonoxynol-9 suppository, solves the problems of the long response ( easy failure of contraception), easy oxidative rancidity, easy discoloration, difficult forming, great irration, and the like existing in the present nonoxynol-9 suppository, thereby having the advantages of short response, stable quality, difficult oxidative rancidity, avirulence, less irritation, no pollution to clothes in use, etc.
CN103479618A Application of Sarcaboside A in medicine for treating dengue virus infection The invention discloses application of Sarcaboside A in a medicine for treating dengue virus infection. The Sarcaboside A can effectively inhibit a dengue virus from proliferating, but has low cytotoxicity, can be further developed to a medicine for treating diseases caused by the dengue virus infection, and has a broad application prospect. The application of the Sarcaboside A in the preparation of the medicine for treating or preventing the dengue virus infection is disclosed for the first time, since the skeleton type of the Sarcaboside A is brand-new, the Sarcaboside A has unexpected strong dengue virus inhibitory activity, has no existing probability of any inspiration given by other compounds, has outstanding substantive characteristics, and meanwhile has the remarkable progress in preventing and treating the dengue virus infection apparently.
US20080125461 Treating, preventing and managing various pulmonary diseases or disorders; with a leukotriene inhibitor such as zafirlukast, montelukast This invention related to methods of treating, preventing and managing various pulmonary diseases or disorders using stereomerically pure (R,R)-formoterol in combination with other pharmacological agents such as leukotriene inhibitors and neurokinin receptor antagonists. Pharmaceutical compositions comprising (R,R)-formoterol and other pharmacological agents are also disclosed.
WO2014060953A1 Process for preparing pemetrexed di potassium and its hydrates The present invention relates to Di potassium (S)-2-(4-(2-(2-amino-4-oxo4,7,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido) pentanedioate (I) and its hydrates useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer. The present invention also relates to a process for preparation thereof.
US20110245345 Topical Treatment Formulation of Natural Ingredients for Enhancing Sexual Response The present invention relates to a topical composition to enhance sexual response. The composition includes L-arginine, trans-resveratrol, and a topical carrier wherein L-arginine is present in an amount not greater than about 10% and trans-resveratrol is present in an amount not greater than about 10% based upon the weight of the total composition. The invention also relates to a method of enhancing sexual response by topically applying the topical composition to the genetalia of a human, and an integrated product including the topical composition, a container for instantaneous delivery, and instructions for use.
CN102283800B Sertaconazole nitrate suppository for treating vaginitis and preparation method thereof The invention discloses a sertaconazole nitrate suppository for treating vaginitis and a preparation method thereof. According to the prescription, the suppository comprises sertaconazole nitrate, a framework material, a matrix, a stabilizing agent, a buffering agent and the like according to a certain proportion. The sertaconazole nitrate suppository has a reasonable formula, slowly releases in vaginas, is not required to be administrated frequently, and can eliminate fungal infection only by one dose of the suppository; and the sertaconazole nitrate suppository has the advantages of appropriate melting point, difficulty in rancidification, extremely good treatment effects on the vaginitis, high pharmacological activity, small toxic or side effects, high cure rate, capability of reducingrecurrence rate and the like, is easy to mold and is extremely suitable for clinical application.
WO2007132900A1 Skin moisturizer and therapeutic agent for dermatitis A therapeutic agent for dermatitis or skin moisturizer containing Pleurotus cornucopiae-derived ceramide as an active ingredient is disclosed. The Pleurotus cornucopiae-derived ceramide has an effect of inhibiting the production of two kinds of chemokines which play an important role in the onset of dermatitis, that is, an effect of inhibiting the production of chemokine CCL1 in a Langerhans cell and an effect of inhibiting the production of dermatitis-inducing chemokine CCL27 in epidermal keratinocytes. Further, the Pleurotus cornucopiae-derived ceramide shows a moisturizing effect and an effect of inhibiting the onset of dermatitis in a dermatitis model mouse. The therapeutic agent for dermatitis or skin moisturizer of the invention has few side effects and can be used for a long period of time.
CN101152143A Solid pharmaceutical composition containing agomelatine The present invention provides a solid medicine combination, which comprises ago cherating as an active ingredient; a non-ionic hydrophilic surfactant which can be accepted by pharmacy. In addition, the present invention is combined with one or a plurality of medicine excipients. The present invention is mainly used for curing depression.
CN103638014A Preparation method of viaminate vitamin E cream The invention belongs to the field of chemical medicine preparation, and particularly relates to a preparation method of a viaminate vitamin E cream. The method comprises the following steps: 1) preparing the following raw materials in parts by weight based on 100 parts in total: 0.1-0.5 part of viaminate, 0.3-0.8 part of vitamin E, 5-10 parts of stearic acid, 5-10 parts of glyceryl monostearate, 0.5-4 parts of wool fat, 0.5-2 parts of albolene, 10-20 parts of glycerin, 0.5-2 parts of sodium dodecyl sulfate, 0.01-0.1 part of preservative and the balance of water; 2) proportionally adding the water-phase raw materials including glycerin, sodium dodecyl sulfate, preservative and water into a water-phase tank to obtain a water phase; 3) proportionally adding the oil-phase raw materials including stearic acid, glyceryl monostearate, wool fat and albolene into an oil-phase tank to obtain an oil phase; 4) transferring the water-phase raw materials and oil-phase raw materials into an emulsifying tank to obtain the cream. The viaminate vitamin E cream prepared by the method provided by the invention is stable in quality and realizes a good curative effect.
CA2649286A1 2-hydroxybenzoic acid derivatives for treating or preventing degenerative and inflammatory diseases The present invention relates to a pharmaceutical composition useful for treating or preventing inflammatory disease and cell damage, and a method for treating or preventing inflammatory disease and cell damage. The present invention uses the 2-hydroxybenzoic acid derivative represented by the specific chemical formula or its pharmaceutically acceptable salt. The compound of the present invention is useful for treating or preventing cell damage and inflammatory disease including gastritis, gastric ulcer, pancreatitis, colitis, arthritis, diabetes, arteriosclerosis, nephritis, hepatitis, Alzheimer's disease, Parkinson' s disease and Lou Gehrig's disease.
CN103041379A Itch relieving and deodorizing insole liquid The invention provides an itch relieving and deodorizing insole liquid, which is characterized by including the following components in part by weight: 3-5 parts of litsea cubeba oil, 3-5 parts of clove oil, 3-5 parts of citionella oil, 3-5 parts of lemon-scented gum oil, 1-2 parts of protease, 50 parts of ethanol, 0.5-2 parts of chlorhexidine dissolved in ethanol, and 100 parts of added 1-2 percent of polyving akohol water solution, that are all stirred and mixed to prepare the itch relieving and deodorizing insole liquid. The itch relieving and deodorizing insole liquid has the characteristics of easily-obtained raw materials, low cost, and excellent itch relieving and deodorizing effects.
CN1679565A Injection of pyritinol hydrochloride and its preparation An injection of pyritinol hydrochloride for treating cerebral injury and improving cerebral metabolism is prepared from pyritinol hydrochloride through including by cyclodextrin and stabilizing for antioxidizing.
CN103263417A Itraconazole isomer and medical application thereof The invention provides a novel itraconazole isomer composition and a method for increasing the therapeutic index of the novel itraconazole isomer composition. The itraconazole isomer composition can be used for improving the selectivity to fungi and endothelial cells and also lowering the toxicity of liver cells. The itraconazole isomer composition provided by the invention is a drug with potential for treating fungi and angiogenesis related diseases, and meanwhile, the side effects caused by taking itraconazole are avoided.
EP1534302A2 Arginine silicate inositol complex and use thereof A method for preventing and treating a variety of disease states and disorders is provided, comprising the administration of an arginine silicate inositol complex to an individual in the presence of medical therapy or absence of medical therapy. Examples of said disease states and disorders include bone and cartilage disorders and cardiovascular disease and its associated micro and macro vascular complications including infections and inflammation of all these diseases in combination or without. Advantageously, the amount of arginine silicate inositol complex administered per day is between about 2 mg/Kg body weight to 2,500 mg/Kg body weight or from a low dose to a higher dose to observe normal metabolic functions and healthy and the delivery is parenteral, oral or intravenous or topical by solid or liquid or both.
CN103610647A Fenbendazole pellet pill The invention discloses a fenbendazole pellet pill, comprising a base pill (1) as a core, a drug layer (2), a coating layer (3) and a color coating layer (4), wherein the drug layer (2) is formed by fenbendazole particles, monostearin, hydroxypropyl methyl cellulose and acrylic resin in a mixing manner; the drug layer (2) is coated on the base pill (1); the coating layer (3) and the color coating layer (4) are orderly coated outwards layer by layer. By adopting the fenbendazole pellet pill, the problems of short half-life period and high administration frequency of the fenbendazole particles are solved, and the defects of the prior art are overcome.
US20100285109 Truncated secretory aspartyl proteinase 2 The present invention relates to a truncated form of the secretory aspartyl proteinase 2 (Sap2), as well as to nucleic acid molecules encoding same. This truncated Sap2 polypeptide (tSap2) is surprisingly stable and devoid of enzymatic activity but retains full immunogenicity upon intravaginal administration and confers full protection against intravaginal challenge by the Candida fungus. The present invention further relates to compositions comprising tSap2 and to the use of tSap2 in the preparation of such compositions.
CN101993474A Glaucocalyxin A derivatives with cyclic octapeptide structure as well as preparation method and application of glaucocalyxin A derivatives The invention discloses a structure of glaucocalyxin A derivatives with cyclic octapeptide structure as well as a preparation method and application of the glaucocalyxin A derivatives in treating cancer. The general formula of the molecular structure of the glaucocalyxin A derivative with cyclic octapeptide structure is shown in the specification, wherein R1 and R2 are -OH or a group shown in the specification, and R3 is a cyclic octapeptide substituent group. The preparation method comprises the following steps: in the presence of tetrahydrofuran and 4-dimethylin pyridine, reacting extracted glaucocalyxin A with succinic acid; in the presence of tetrahydrofuran and dichloroethane, reacting the obtained succinate of glaucocalyxin A with N-hydroxyl succinimide to obtain the intermediate product; and finally, in the presence of tetrahydrofuran and phosphate buffer, carrying out derivatization reaction on the obtained intermediate product with cyclic octapeptide, thereby obtaining the glaucocalyxin A derivatives with the cyclic octapeptide structure.
US20130011477 Stable Pharmaceutical Composition of Imatinib The present invention relates to a compressed film-coated tablet comprising imatinib its pharmaceutically acceptable salts there of in an amount of more than 80% based on the total weight of the finished dosage form.
WO2012045803A1 Co-crystals and salts of ccr3-inhibitors This invention relates to co-crystals and salts of CCR3 inhibitors of formula (1), pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.
WO2012061698A3 Compounds useful as modulators of trpm8 The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
CN102342892A Cosmetic composition containing a particular water, and use thereof as a depigmenting or anti-ageing agent The invention relates to the use, in a cosmetic or dermatological composition, of a particular water having a pH of between 7.8 and 10 and a total dissolved solids (TDS) concentration of between 10 and 250 mg/l. The invention also relates to a cosmetic or dermatological composition containing this water. The invention relates in particular to a treatment method intended for preventing or delaying the appearance of the effects of intrinsic and/or extrinsic ageing of the skin, or for slowing down the effects thereof; for preventing or reducing pigmentary spots on the skin, or the coloration of hyperpigmented areas of skin; for reducing the pigmentation of the periphery of depigmented areas; for improving the uniformity of the skin coloration; or for lightening the complexion of the skin.
US6982075 Administering a pulmonary surfactant preparation, including a phosphatide and/or a surfactant protein to artificially respirate a patient suffering from a toxic oxygen concentration; side effect reduction The invention describes the novel use of pulmonary surfactant preparations in the artificial respiration of patents with toxic oxygen concentrations.
EP1451151B1 Hydroperylene derivatives The invention relates to compounds of formula (I) which are suitable for producing medicaments used for the prophylaxis and therapy of illnesses characterised by increased blood platelet aggregation.
CN1813793A Dermatan sulfate and its derivative oral formulation and preparing method The present invention discloses an oral preparation of dermatan sulfate and its dervarive. Said oral preparation contains the following components: (by weight portion) 25-100 portions of dermatan sulfate or its derivative, 10-30 portions of taurocholic salt, 0.5-1.0 portion of taurine, 5-10 portions of oleic acid and 5-10 portions of lecithine. Said oral preparation can be made into various dosage forms. Besides, said invention also provides the concrete steps of its preparation method. Said oral preparation has the strong action for resisting thrombosis, inflammation-resisting activity and good tumor-resisting activity.
WO2008145789A1 Use of compounds derived from benzamidine methanesulphonate or a pharmaceutically acceptable salt thereof, for example imatinib mesylate, for the preparation of a drug for the treatment of neurodegenerative niemann-pick c disease (npc) The invention relates to the use of imatinib mesylate for the treatment of metabolic disorders characterised by neurodegeneration, in particular a metabolic disorder characterised by an inability to metabolize lipids, such as in patients with Niemann-Pick C disease. More specifically, the invention relates to a treatment for neurodegenerative diseases, comprising the delivery of a therapeutically effective quantity of a compound derived from benzamidine methanesulphonate or a pharmaceutically acceptable salt thereof. The invention also relates to a treatment for neurodegenerative diseases, comprising the delivery of a therapeutically effective quantity of a compound derived from imatinib mesylate or a pharmaceutically acceptable salt thereof.
CA2789276A1 New signaling molecule involved in ultraviolet damage to skin The present invention includes a method of detecting ultraviolet radiation (UVR)-induced skin damage in a mammal. The present invention also includes a method of identifying a mammal at risk of developing U VR-induced skin damage, photoaging, or photocarcinogenesis. The present invention further includes a method of inhibiting UVR-induced skin damage in a mammal at risk of developing U VR-induced skin damage. The present invention also includes a method of reducing the level of Syk kinase in the skin of a mammal. The present invention further includes methods of treating or diagnosing a disease associated with a change of Syk kinase expression in the skin in a mammal.
US20130059892 Compositions and Methods for Cancer Detection and Treatment Disclosed herein are compositions and methods for cancer detection and treatment. Compounds that inhibit PRMT5 are contemplated, as are pharmaceutical compositions comprising a therapeutically effective amount of at least one PRMT5 inhibitor. In some embodiments pharmaceutical compositions further comprising at least one HDAC inhibitor are contemplated. Methods of treating disorders in a mammal by inhibiting PRMT5 by administering to a mammal, a therapeutically effective amount of a PRMT5 inhibitor are also disclosed.
US20080311102 Nucleic acid molecule that encodes the MGAT-X1 protein; pharmaceutical composition containing the nucleic acid or its expression vector The present invention is directed to a polynucleotide sequence of a novel acylglycerol acyltransferase-like protein MGAT-X1. The invention also provides the human MGAT-X1 associated with the dermatological diseases, urological diseases, muscle-skeleton disorders, hematological diseases, cancer, reproduction disorders, neurological diseases, metabolic diseases, cardiovascular diseases or gastroenterological diseases. The invention also provides assays for the identification of compounds useful for the modulation of dermatological diseases, urological diseases, muscle-skeleton disorders, hematological diseases, cancer, reproduction disorders, neurological diseases, metabolic diseases, cardiovascular diseases or gastroenterological diseases for treating of such diseases associated with expression of the MGAT-X1. The invention also features compounds which bind to and/or activate or inhibit the activity of MGAT-X1 as well as pharmaceutical compositions comprising such compounds.
EP1051193B1 Anhydrous topical skin preparation comprising ketoconazole The present invention provides anhydrous compositions for topical delivery of a medicament comprising (A) a penetration enhancer/solvent selected from the group consisting of alcohol, propylene glycol, or a combination thereof; (B) a humectant/solvent selected from the group consisting of polyethylene glycol, glycerin, sorbitol, xylitol, or any combination of any of the foregoing; and (C) an anhydrous vehicle. In an alternate embodiment, the present invention provides anhydrous compositions for topical delivery of a medicament which comprise (A) a penetration enhancer/solvent selected from the group consisting of alcohol, propylene glycol, or a combination thereof; (B) a humectant/solvent selected from the group consisting of polyethylene glycol, glycerin, sorbitol, xylitol or any combination of any of the foregoing; (C) an anhydrous vehicle; and (D) a medicament. Also provided are methods for topically delivering a medicament to an animal, such as a mammal or a human patient, in need of the medicament by topically administering to the animal the compositions of the present invention.
CA2833942A1 Novel compound useful for the treatment of degenerative and inflammatory diseases A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed,as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolite thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hyper secretion of IL6.
CN102657660A Application of total triterpenes in preparing drugs inhibiting angiogenesis The invention relates to application of total triterpenes in preparing drugs inhibiting angiogenesis. The application has the advantages that novel application of the total triterpenes in extractive of Actinidia chinensis roots is provided. An experiment proves that the total triterpenes 1,2,3,4 have remarkable inhibiting effect on multiplication of human umbilical vein endothelial cells (HUVEC) and canaliculization of HUVEC, have anti-angiogenic activity, and can serve as angiogenesis inhibitors. By means of the application of the total triterpenes in preparing the drugs inhibiting the angiogenesis, the anti-angiogenesis effect of the total triterpenes in the extractive of Actinidia chinensis roots is firstly found out, and the total triterpenes can serve as the angiogenesis inhibitors to be applied to treat new blood vessel dependence and new vessel related diseases including tumors, arthritis, skin and eye diseases, atherosclerosis and the like.
CN102040591A 7-phenyl quinolone compounds The invention belongs to the technical field of medicaments, and in particular relates to 7-phenyl quinolone compounds shown as a general formula (I), and pharmaceutically acceptable salt, solvate and stereoisomers thereof, wherein R<1>, R<2>, R<3>, R<4>, R<5> and n are defined in the specifications. The invention also relates to a method for preparing the compounds, medicinal preparations containing the compounds, and application of the compounds to the preparation of medicaments for treating and/or preventing infectious diseases.
US20100240766 Agent for Improving Carcass Performance in Finishing Hogs A food supplement for finishing hogs containing astaxanthin is described.
CA2481078C Method and compositions for the synthesis of bch-189 and related compounds The present invention relates to a method of preparing BCH-189 and various analogs of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds, .beta.-BCH-l89 and related compounds. Furthermore, the stereochemistry at the nucleoside 4' position can be controlled to produce enantiomerically-enriched .beta.-BCH-189 and its analogs.
US7217840 Method for preparing 1,3,5-triaminobenzene and hydrolyzing it into high-purity phloroglucinal The invention concerns a method for method for preparing 1,3,5-triaminobenzene, characterized in that it comprises a step which consists in amination of a compound of formula (I), wherein: A represents a halogen atom or a NH2 group; X1 and X2, identical or different, represent each a halogen atom, the amination step being carried out in the presence of ammonia and a catalyst selected from the group consisting of copper salts, cupric and cuprous oxides or mixtures thereof at a temperature ranging between 150° C. and 250° C. and at a pressure higher that 35 bars
WO2003051287A3 Topical compositions and methods for treatment of adverse effects of ionizing radiation Compositions and methods for the prevention, reduction or treatment of adverse effects due to exposure to ionizing radiation, including at least one flavonoid and at least one non-flavonoid antioxidant, optionally formulated in a acceptable carrier for a topical composition. The composition of the present invention may further include optional ingredients such as selenium, selenium compounds, anti-inflammatories, organic germanium compounds, compounds that regulate cell differentiation, Korean ginseng, American ginseng, Siberian ginseng and B-complex vitamins. A method for the topical administration of the composition in accordance with the present invention for the purpose of reducing, treating or preventing adverse effects caused by ionizing radiation involves topically administering a safe and effective amount of the composition of the invention an area of skin, which has been, is being or will be exposed to ionizing radiation. The compositions and methods can be employed to reduce, treat or prevent radiation injury caused by a wide variety of types of exposure to ionizing radiation.
EP1919304B1 Compositions and methods for improving functional vascular integrity, cellular survival and reducing apoptosis after an ischemic episode in the brain Compositions and methods for enhancing vascular integrity in animals are disclosed. The compositions and methods, which utilize long chain polyunsaturated fatty acids and nitric oxide releasing compounds are also effective for reducing ischemia-induced brain injury in an animal.
US7312212 Bactericides for infrections in man Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
EP1802643A1 Antiviral oligonucleotides Random sequence oligonucleotides that have antiviral activity are described, along with their use as antiviral agents. In many cases, the oligonucleotides are greater than 40 nucleotides in length and include chemical modifications, such as modified internucleotidic linkages and modifications at the 2'-position of the ribose moieties. Also described are uses for the prophylaxis or treatment of a viral infection in a human or animal, and use for the prophylaxis or treatment of cancer caused by oncoviruses in a human or animal. The uses typically involve administering to a human or animal in need of such treatment, a pharmacologically acceptable, therapeutically effective amount of at least one oligonucleotide that act by a sequence independent mode of action.
EP2760444A1 Cannabinoid carboxylic acids, salts of cannabinoid carboxylic acids, and the production and uses of same The invention relates to a compound selected from the group consisting of all stereoisomers and their mixtures of the compounds of general formulas (1)-(4), in which R1 is a straight-chained, branched or cyclic hydrocarbon group with up to 12 C-atoms and X+ is selected from the group consisting of H+, NH4 +, mono, di or trivalent metal cations, NH4 +, primary, secondary, tertiary or quaternary organic ammonium ions with up to 48 C-atoms, which can carry even more functional groups, hydrazinium ion (N2H5 +), hydroxylammonium ion (NH3OH+), guanidinium ion (CN3H6 +), and organic derivatives of (N2H5 +), NH3OH+, and CN3H6 +, which can carry even more functional groups, and similar. A method is also provided for producing these compounds, comprising the following steps: producing synthetic cannabinoid carboxylic acids in a chemical reaction, or extracting natural cannabinoid carboxylic acids from plant material or cell cultures of Cannabis sativa, and adding a suitable inorganic base, a suitable organic base and/or a suitable inorganic or organic salt in a suitable solvent, to the cannabinoid carboxylic acids or cannabinoid carboxylic acid-rich extracts produced in this manner.
WO2013075823A1 Transdermal therapeutic system comprising rotigotine and crystallization inhibitor The present invention relates to an inventive transdermal therapeutic system (TTS) comprising rotigotine, a pharmaceutically acceptable adhesive comprising styrene butadiene block copolymer and a crystallization inhibitor, an inventive matrix with an extended release of rotigotine suitable for a transdermal therapeutic system, an inventive production method of a respective matrix or a respective TTS comprising rotigotine, as well as uses of the inventive matrix and the inventive TTS.
US20080305153 Antibacterial Sol-Gel Coating Solution, Method for Preparing Antibacterial Sol-Gel Coating Solution, Antibacterial Articles, and Method and Equipments for Preparing Antibacterial Articles The invention relates to an antibacterial sol-gel coating solution, a process for preparing the antibacterial sol-gel coating solution, an antibacterial article, and a process and an apparatus for producing the antibacterial article. Said antibacterial sol-gel coating solution comprises a. at least one substance selected from the group consisting of Ti or Si-containing compounds capable of hydrolyzing to form a base film; b. a regulating agent capable of regulating the hydrolysis rate of the Ti or Si-containing compounds; c. an organic solvent; d. water; and e. at least one soluble compound of antibacterial metal selected from the group consisting of Ag, Cu, Mg, Zn, Sn, Fe, Co, Ni, and Ce; wherein a, b and a portion of c are first mixed to form a solution I, d and the rest of c are then mixed and added into solution I to form a dispersion II, and then e is added into dispersion II to form the antibacterial sol-gel coating solution.
US7078209 Fused nitrogen heterocyclic compounds; treating fungal diseases The present invention relates to compounds useful as inhibitors of CAK, compositions thereof. The present invention also relates to methods using the compositions for treating CAK-mediated diseases, such as fungal infections.
WO2007021839A2 Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.
EP1531158A1 Lipid A and topic, in particular cosmetic, composition thereof Lipid A compounds (I) are new. - Lipid A compounds of formula (I) are new: - AG1 = 3-hydroxydecanoyl; - AG2 = 3-dodecanoyloxydecanoyl; - R = H or PO(OR')2; - R' = H, M, 1-6C (un)saturated alkyl, phenyl or benzyl; - M = an (in)organic, amine or phosphoethanolamine cation. - Independent claims are included for: - (1) a composition for topical application to the skin, comprising a compound (I) in a cosmetically acceptable carrier; - (2) a cosmetic skin treatment comprising topical application of the above composition.
CA2206366C Substituted 2-naphthoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them Substituted 2-naphthoylguanidines of the formula I (see formula I) are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. They also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the production of ischemically induced cardiac arrhythmias.
CN103638022A Application of penehyclidine hydrochloride in treatment of gastric ischemia caused by infectious shock The invention discloses application of penehyclidine hydrochloride in treatment of gastric ischemia caused by an infectious shock. Microcirculation can be effectively improved, tissue perfusion is increased, and especially, the penehyclidine hydrochloride has a significant effect on the gastric ischemia caused by the infectious shock.
US6939871 Central nervous system disorders including depression and/or anxiety; 5-HT1 type receptor and/or serotonin reuptake inhibition activity The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar is phenyl, naphthyl, a monocyclic heteroaromatic group or a bicyclic heteroaromatic group, said Ar group being optionally substituted by 1-4 substituents, which may be the same or different, and which are selected from the group consisting of: halogen, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-6alkyl, trifluoromethanesulfonyloxy, pentafluoroethyl, C1-6alkoxy, arylC1-6alkoxy, C1-6alkylthio, C1-6alkoxyC1-6-alkyl, C3-7cycloalkylC1-6alkoxy, C1-6alkanoyl, C1-6alkoxycarbonyl, C1-6alkylsulfonyl, C1-6alkylsulfinyl, C1-6alkylsulfonyloxy, C1-6alkylsulfonylC1-6alkyl, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-6alkyl, C1-6alkylsulfonamido, C1-6alkylamido, C1-6alkylsulfonamidoC1-6alkyl, C1-6alkylamidoC1-6alkyl, arylsulfonamido, arylcarboxamido, alkylsulfonamidoC1-6alkyl, arylcarboxamidoC1-6alkyl, aroyl, arolC1-6alkyl, arylC1-6alkanoyl, a group R<3>OCO(CH2)s, R<3>CON(R<4>)(CH2)s, R<3>R<4>NCO(CH2)s or R<3>R<4>NSO2(CH2) where each of R<3> and R<4> independently represents a hydrogen atom or C1-4alkyl or R<3> and R<4> form part of a C3-6azacyloalkane or C3-6(2-oxo)azacycloalkane ring and s represents zero or an integer from 1 to 4, and a group Ar<1>Z, wherein Z represents a single bond, O, S or CH2 and Ar<1> represents a phenyl or a monocyclic heteroaromatic group, said Ar<1> group being optionally substituted by 1-3 substituents, which may be the same or different, and which are selected from the group consisting of a halogen, hydroxy, cyano, trifluoromethyl, C1-6alkyl, C1-6alkoxy or C1-6alkanoyl; when Ar is a phenyl or a monocyclic heteroaromatic group, substitutents positioned ortho to one another may be linked to form a 5- or 6-membered ring; R<1> is hydrogen, C1-6alkyl, C3-6alkenyl, C3-6alkynyl or arylC1-6alkyl; R<2> is halogen, C1-6alkyl, cyano, CF3, C1-6alkanoyl, C1-6alkoxy or hydroxy; X is CH or N; Y is a single bond, O, or C═O; p is 0, 1 or 2; r is 0, 1, 2 or 3; m is 2, 3 or 4; n and q are independently 1 or 2. Processes for preparing the compounds, pharmaceutical compositions containing them and their use as medicaments for various CNS disorders, including deression and/or anxiety, are also disclosed.
CN102617596A Dimeric sesquiterpene compound Hippolide I, its preparation method and its purpose The invention relates to the medicine technical field, more specifically relates to a dimeric sesquiterpene compound Hippolide I separated from marine animal sponge, its preparation method and its purpose. sponge is extracted by ethanol according to a routine percolation method, concentrated, separated and purified to obtain Hippolide I, its molecular formula is C24H35O2; the preparation method has the advantages of simple technology, high yield and stable property, the prepared preparation has the advantages of stable quality, simple quality control and low production cost, and is convenient for industrial production; the compound possesses strong pharmacological effect, and can be used for anti-tumor, anti-diabetes and anti-obesity, the compound Hippolide I provides a novel medicine source and safe raw material for preventing, diagnosing, detecting, protecting, treating and researching anti-tumor, anti-diabetes, anti-obesity and directly relative diseases.
CA2695782A1 Prostate perform Relates to a novel formulation consisting of herbs and nutraceuticals for the relief of symptoms related to Prostatitis. This relates to the use of a softgel formula of herbs and nutraceuticals to achieve treatment of symptoms associated with Prostatitis. A novel formulation consisting of herbs and nutraceuticals for the relief of symptoms related to Prostatitis.
US20110306585 Metal Complexes of N-Heterocyclic Carbenes The present invention generally relates to metal complexes of N-heterocyclic carbenes that contain one or more additional active moieties and/or groups therein. In one embodiment, the present invention relates to metal complexes of N-heterocyclic carbenes that contain an anti-fungal and/or anti-microbial moiety and/or group in combination with one or more additional active moieties and/or groups selected from fluoroquinolone compounds or derivatives thereof; steroids or derivatives thereof; anti-inflammatory compounds or derivatives thereof; anti-fungal compounds or derivatives thereof; anti-bacterial compounds or derivatives thereof; antagonist compounds or derivatives thereof; H2 receptor compounds or derivatives thereof; chemotherapy compounds or derivatives thereof; tumor suppressor compounds or derivatives thereof; or C1 to C16 alkyl heteroatom groups where the heterotatom is selected from S, O, or N. In still another embodiment, the present invention relates to metal complexes of N-heterocyclic carbenes that contain an anti-fungal and/or anti-microbial moiety and/or group in combination with two or more additional active moieties and/or groups selected from fluoroquinolone compounds or derivatives thereof; steroids or derivatives thereof; anti-inflammatory compounds or derivatives thereof; anti-fungal compounds or derivatives thereof; anti-bacterial compounds or derivatives thereof; antagonist compounds or derivatives thereof; H2 receptor compounds or derivatives thereof; chemotherapy compounds or derivatives thereof; tumor suppressor compounds or derivatives thereof; or C1 to C16 alkyl heteroatom groups where the heterotatom is selected from S, O, or N.
US20060235054 e.g. 3-substituted 5-(4-fluorophenyl)-4-(4-pyridyl)imidazole-2-thione; immunomodulating and cytokine-release-inhibiting action; antiinflammatory agent The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2 R3 and m are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.
CN1943562A Ubenimex dispersion tablet and its preparing method The invention relates to ubenimex disket and its process, a composition disket comprising such as active ubenimex, disintegrating agent, filler, suspending agent bond, glidant, corrigent. Said ubennimex disket is convenient for medication, suitable for the old and small children and patient with swallowing difficulties.
CN101496929A Nose-protecting device for killing bacteria and virus The invention relates to a bacteria and virus killing nose protector, which can quickly and effectively kill bacteria and viruses. The technical proposal is that the bacteria and virus killing nose protector is characterized in that the bacteria and virus killing nose protector is provided with a body capable of being plugged into a nostril; and the body is made of medical sponge and is dipped with liquid medicine. The bacteria and virus killing nose protector has short treatment cycle, takes effect quickly in killing the bacteria and the viruses in the nasal cavity, can effectively kill the following harmful bacteria in two minutes: Staphylococcus aureus, colon bacillus, Candida albicans and the like, can effectively kill the viruses such as Coxsackie virus and partial linear virus, and has a killing rate of 100 percent.
WO2008000643A1 Benzimidazole derivatives, method for the production thereof, their use as fxr agonists and pharmaceutical preparations containing the same The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.
EP1399138B1 Method for the production of solid formulations of sodium 3-hydroxy-3-methylbutyrate Solid formulations of sodium 3-hydroxy-3-methylbutyrate are produced by the hydrolysis of 4,4-dimethyl-2-oxetanone with aqueous sodium hydroxide to give a solution of sodium 3-hydroxy-3-methylbutyrate and the solution obtained thus is absorbed onto synthetic silicic acid. Said formulations are lightly hygroscopic and easily handled.
US20100204199 Cyclic 11-beta hydroxysteroid dehydrogenase type i inhibitors Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.
CN101475571B Beta-carbolines cell cycle protein related kinase 2 inhibitor and use thereof The invention relates to the field of pharmacochemistry, in particular to beta-carboline alkaloids (I), and methods for preparing the same, pharmaceutical compositions containing the same and the pharmaceutical uses of the same, especially the use of the compounds as cyclin-dependent kinase 2 inhibitors.
US20100261712 Hematopoietic neoplasm chemotherapy A method and medicament for treating mixed lineage leukemia; translocated mixed lineage leukemia; translocated mixed lineage leukemia based acute myelogenous leukemia; translocated mixed lineage leukemia based acute lymphoid leukemia; a non-MLL based chronic myeloproliferative disorder, or non-MLL based acute lymphoid leukemia is provided.
US20090082429 Antimicrobial Compositions and Methods of Use A catechin is modified in at least one position (most preferably in the 3-position of the C-ring) to increase its lipophilicity. Contemplated catechins are demonstrated to have significantly improved antibacterial properties, likely due to catastrophic membrane damage.
CN101898966A Bromine and piperazine ring-containing Artemisia rupestris L. keto ester derivative as well as preparation method and application thereof The invention relates to a bromine and piperazine ring-containing Artemisia rupestris L. keto ester derivative as well as a preparation method and application thereof. The preparation method of the derivative comprises the following steps of: synthesizing a midbody omega-bromoalkoxyl Artemisia rupestris L. keto ester derivative 2a-2g under the action of catalyst tetrabutyl ammonium bromide by using Artemisia rupestris L. keto acid and 1,omega-dibromoalkyl as raw materials; under the action of anhydrous potassium carbonate and in the presence of acetonitri used as a solvent, reacting the derivative 2a-2g with 1-methylpiperazine to obtain an omega-(4-methylpiperazainyl)-alkoxy Artemisia rupestris L. keto ester derivative 3a-3g, or reacting the derivative 2a-2g with 1-phenylpiperazine to obtain an omega-(4-phenylpiperazainyl)-alkoxy Artemisia rupestris L. keto ester derivative 4a-4g; and carrying out in-vitro A type H3N2, H1N1 and influenza B virus activity resistant test on the synthesized derivative. Results indicate that a compound which is 2g has better inhibiting effect on the HINI influenza A virus, the compounds which are 3c, 3d, 3g and 4g have better inhibiting effect on H3N2and H1N1 influenza A virus, and the compound which is 3d has better inhibiting effect on the influenza B virus.
US20070087388 G protein coupled receptor The invention provides nucleic acid encoding a G protein coupled receptor (adenine binding GPCR) with specificity for adenine, isolated adenine binding GPCR, assay and treatment methods utilising the same.
CA2214793C Novel intermediates and process for the manufacture of camptothecin derivatives (cpt-11) and related compounds This invention discloses and claims novel intermediates and procedures for the synthesis of camptothecin derivatives, such as irinotecan, and other compounds related to the synthesis of CPT-11 of formula (I). Related procedures and compounds are also disclosed, such as a novel method of making mappicine of formula (II).
US7790680 Hemophilia biodrug recombinant porcine factor 8 formulation with replacement for albumin stabilizer, which may carry risk of prions; surfactant such as polysorbate, calcium chloride, sucrose, sodium chloride, trisodium citrate, and a buffer devoid of amino acids The invention relates to a stable solid pharmaceutical composition comprising factor VIII. Such a composition is devoid of amino acids and comprises: (a) factor VIII; (b) a surfactant; (c) calcium chloride; (d) sucrose; (e) sodium chloride; (f) trisodium citrate; and (g) a buffer devoid of amino acids; and has a pH from 6 to 8 prior to lyophilization and after reconstitution in water for injection. The invention also relates to the liquid pharmaceutical composition obtainable after dilution of said stable solid pharmaceutical composition with sterile water optionally containing sodium chloride.
US7129379 3-amino-propoxphenyl derivatives (l) Compounds of formula (Ia) as potent, β1-specific beta blockers with a short duration of action in the systemic circulation, wherein R is 3′,4′-dimethoxyphenyl, R1 is hydrogen, and R2 is selected from methyl, ethyl, propyl, isobutyl and isopropyl; or R is 3′,4′-dimethoxyphenyl, R1 is selected from fluorine, chlorine and bromine, and R2 is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; of R is 4′-methoxyphenoxy, R1 is selected from hydrogen, fluorine, chlorine and bromine, and R2 is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; or R is 3′,4′-dimethoxyphenyl, R1 is cyano, and R2 is cyclopropylmethyl; or R is 4′-methoxyphenoxy, R1 is cyano, and R2 is isobutyl; and physiologically acceptable hydrolysable derivatives thereof having the hydroxy group in the 2-position of the 3-aminopropoxy side chain in esterified form, in their racemic and optically active forms, and their pharmaceutically acceptable acid addition salts.
WO2012027825A1 Method of treating dopamine-related neuropsychiatric disorders The use of a therapeutically effective amount of a pyrrolidinacetamide analogue, such as POPOA, for treating dopamine realated neuropyschiatric disorders such as schizophrenia, autism spectrum disorder (ASD), bipolar disorder, Alzeimer's disease, Lewy body disease and drug or behavioral addications.
CN1974591A SiRNA expression template for treating liver necrosis and liver fibrosis The present invention relates to one kind of siRNA expression template for treating liver necrosis and liver fibrosis. The present invention includes designing one siRNA expression template to break the signal transduction path of TBR mediating and transforming growth factor beta (TGF beta), and inserting the template into siRNA expression vector pRNAT-U6.1/Neo to obtain the recombinant plasmid pRNA-TBR I. It is proved through transfecting 3T3 fibroblast, MTT screening and animal experiment that the recombinant plasmid pRNA-TBR I can break liver fibrosis course and improve liver's function effectively. The present invention opens one new way for developing genetic medicine for treating chronic hepatitis and blood fluke liver necrosis.
WO2008130944A1 Solid phase syntheses of amino pyrimidine compounds The invention methods for the solid-phase syntheses of amino pyrimidine compounds, such as imatinib and analogs thereof.
DE102004009835A1 New 4-heterocyclyl-benzamide derivatives, useful as antithrombotic agents for treating or preventing e.g. deep vein thrombosis or reocclusion after angioplasty, are inhibitors of factor Xa and other serine proteases N-substituted 4-heterocyclyl-benzamide derivatives (I), their tautomers, enantiomers, diastereomers (and mixtures) and salts are new. - N-substituted 4-heterocyclyl-benzamide derivatives of formula (I), their tautomers, enantiomers, diastereomers (and mixtures) and salts are new. - A = heterocyclic group; - R1 = hydrogen, fluoro, chloro, bromo, 1-3C alkyl (optionally (per)fluorinated), 2-3C alkenyl or alkynyl, nitro, amino, 1-3C alkoxy or mono-, di- or tri-fluoromethoxy; - R2 = hydrogen, chloro, bromo or 1-3C alkyl; - R3 = hydrogen or a substituent; - R4 = hydrogen or 1-3C alkyl, or R3 and R4 together complete 3-7C cycloalkyl in which one methylene may be replaced by imino, 1-3C alkylimino, acylimino or sulfonylimino; - R5 = hydrogen or 1-3C alkyl; - B = fused heterocyclic group of formulae (Bi), (Bii) and (Biii); - n = 1 or 2; - R7 = hydrogen, 1-3C alkyl (optionally substituted by carboxy or 1-3C alkoxycarbonyl), hydroxy, 1-5C alkoxycarbonyl, amino or 1-3C alkylamino; - R8 = hydrogen, fluoro, chloro, bromo, iodo, 1-3C alkyl (optionally (per)fluorinated), 2-3C alkenyl or alkynyl, hydroxy, 1-3C alkoxy, trifluoromethoxy, amino, nitro or cyano. - The full definitions are given in the DEFINITIONS (Full Definitions) Field. - ACTIVITY - Thrombolytic; Anticoagulant; Antiulcer; Cerebroprotective; Cardiant; Cytostatic; Antiarthritic; Antirheumatic. - No biological data is given. - MECHANISM OF ACTION - (I) are inhibitors of factor Xa and/or related serine proteases (e.g. thrombin, urokinase, factors VIIa, IXa, XIa and XIIa).
EP1809639B1 8a, 9-dihydro-4a-h-isothiazolo[5,4-b] quinoline-3, 4-diones and related compounds as anti-infective agents The invention provides compounds and salts of Formula I and Formula II which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables n, m, p, RA, RB, A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and /or selective inhibitors of bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in eukaryotes.
EP1656138A2 Substituted cycloalkyamine derivatives as modulators of chemokine receptor activity The present application describes modulators of MCP-1 of formula (I) or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
CN102085174A Benzaconine transdermal gel having effects of relieving pain and resisting inflammation The invention relates to a benzaconine transdermal gel having effects of relieving pain and resisting inflammation. The gel comprises the following components in percentage by weight: 0.1 to 10 percent of benzaconine, 2 to 30 percent of transdermal penetrating agent, 60 to 95 percent of solvent and 1 to 20 percent of gel matrix. The gel is prepared by dissolving the benzoyl aconine transdermal, the transdermal penetrating agent and the solvent in the gel matrix. The benzaconine keeps the biological activities of relieving the pain and resisting the inflammation of aconitine, the toxicity is obviously reduced, medicaments can directly reach lesion sites through transdermal medicament delivery, and the safety is further improved. The benzaconine and the aconitine have basically consistent transdermal penetrating behaviors, can be directly penetrated into skin and have quick response. Animal medicinal effect tests in which the benzaconine is prepared into the gel show that the gel has obvious and exact pharmacological effects of relieving the pain and resisting the inflammation.
US7956050 Psychological disorders; analgesics; hyperactivity; eating disorders The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
US6852720 Thiazol-2-yl-imine compounds as PDE-7 inhibitors A compound selected from those of formula (I): wherein: R1, R2, R3 are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as inhibitors of phosphosdiesterase-7.
CA2140106C Method of treating hyperproliferative vascular disease A method of preventing or treating hyperproliferative vascular disease in a mammal consists of administering an effective amount of a compound of the formula I or II (see formula I, II) to said mammal.
EP1625123A2 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists The present invention encompasses compounds of Formula (I): as well as the pharmaceutically acceptable salts thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
WO2006043515A1 Pyrimidine-5-carboxylic acid derivative Disclosed are a novel pyrimidine-5-carboxylic acid derivative having PPARϜ modulating activity and a pharmacologically acceptable salt thereof. Specifically disclosed are a pyrimidine-5-carboxylic acid derivative represented by the general formula (1) below and a salt thereof. [Example: 4-anillino-6-(benzylthio)-2- (methylthio)pyrimidine-5-carboxylic acid]
US20110212895 Treatment of Cognitive and Learning Impairment Constitutive activators of Rho GTPases are useful in treating learning an cognitive disorders.
WO2006037346A1 Pharmaceutical compositions comprising fenofibrate and simvastatin Pharmaceutical compositions in particulate form or in solid dosage forms comprising a combination of a reduced or low dose of fenofibrate and the HMG CoA reductase inhibitor simvastatin or a pharmaceutically active salt thereof. Simvastatin is optionally provided as a controlled release or a delayed release formulation, which may result in a maintained LDL-lowering effect at a reduced dosage. Fenofibrate is provided in a formulation being bioequivalent to commercially available Antara® capsules, or exhibiting increased bioavailability as compared therero, and also reduced food effect.
WO2013114231A1 Treated apertures A personal care article comprising a nonwoven fluid permeable topsheet having a body-facing surface and an opposing backside surface, a fluid impermeable backsheet and at least one intermediate layer disposed therebetween, wherein said fluid permeable topsheet comprises apertured holes wherein at least 10% of the aperture holes are treated with a hydrophilic treatment agent.
WO2012030647A1 Treatment of cystic fibrosis using calcium lactate, leucine and sodium chloride in a respiraple dry powder The invention relates to a methods for treating cystic fibrosis, comprising administering an effective amount of a calcium salt formulation to the respiratory tract of an individual with cystic fibrosis. The calcium salt formulation is can be a dry powder formulation.
US20050287195 Transdermal drug delivery systems In a method of manufacturing such a system, an active substance is dissolved in a ratio less than saturation level in a solvent which is also a skin penetration enhancer. The system is coated as a layer onto a siliconized release paper and laminated onto a backing strip.
US20100168203 Adenylyl cyclases as novel targets for antibactrial interventions The present invention relates to a method of preventing or treating a disease caused by bacterial infection by administering an effective amount of a modulator of bacterial adenylyl cyclase. The invention also provides pharmaceutical compositions useful for preventing or treating a disease, with the compositions containing a therapeutically effective amount of a modulator of bacterial adenylyl cyclase. The invention also provides screening methods for identifying selective modulators of bacterial adenylyl cyclase that do not substantially modulate adenylyl cyclase of the subject. The invention also provides methods for culturing bacterial pathogens and methods for inducing the pathogenic state in vitro.
CN102988394A Application of Houttuynoid D in preparation of medicine for treating acute gout The invention provides application of Houttuynoid D in medicines, and in particular relates to an application of Houttuynoid D in preparation of a medicine for treating acute gout. The experimental research proves that the Houttuynoid D has a function of protecting an acute gout model of urate-caused human vascular endothelial cell damage and suppresses the ICAM-1; and therefore, the Houttuynoid D can be used for preparing a medicine for treating acute gouty inflammation. The application of Houttuynoid D in preparation of medicine for treating acute gout is disclosed for the first time, and because the framework type belongs to a novel framework type, the prevention and treatment activity on the acute gout is unexpectedly high, the possibility that other compounds give enlightenment is avoided, and the Houttuynoid D has outstanding substantial characteristics and has obvious progress in prevention and treatment of the acute gout.
US20110269823 Compositions And Methods For Inhibiting Expression Of The HAMP Gene The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of the HAMP gene (HAMP gene), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of the HAMP gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by HAMP gene expression and the expression of the HAMP gene using the pharmaceutical composition.
CN101336959B Composition with acne-removal function A composition with acne removing effect is mainly prepared from the following raw materials of (by weight parts): rosemary 0.5-10 and pine needles 0.5-10. Natural acne removing components such as lavender oil and tea tree oil and/or chemical acne removing components such as vitamin B6 and allantoin can also be added. The composition can be made into pharmaceuticals or cosmetics together with pharmaceutically or cosmetically-acceptable adjuvants; has effects of inhibiting skin grease secretion, inhibiting acne growth, relieving inflammations, killing Corynebacterium acnes, removing acne, and caring skin; and has the advantages of easily accessible raw materials, low production cost, good safety, and no toxic and adverse effects.
WO2010011975A1 Oxymatrine compositions and use thereof for treating and preventing chronic infectious diseases Compositions and methods for treating chronic infectious diseases using substantially pure oxymathne or pharmaceutically acceptable salts or esters thereof are disclosed. In one embodiment described herein, the chronic infectious disease is chronic fatigue syndrome. Further described are compositions having an anti-infective amount of substantially pure oxymathne or pharmaceutically acceptable salts or esters thereof.
CA2215319C Compositions comprising nicotinylalanine and an inhibitor of glycine conjugation or vitamin b6 This invention relates to methods and compositions comprising nicotinylalanine, and/or related analogues, and an inhibitor, such as aspirin, of glycine conjugation, which are useful for inhibiting cellular poly-(ADP-ribose) synthetase in vitro and/or in vivo. This enzyme is activated in a variety of toxic and pathological conditions and is inhibited by nicotinamide. B6 may also be present in the compositions of this invention in place of, or in addition to the inhibitor of glycine conjugation. Such pathological conditions include for example, neurodegenerative disorders, viral infections, autoimmune diseases and cancer. Accordingly, this invention relates to methods of reducing cellular toxicity and treating such diseases by increasing cellular nicotinamide using the methods and compositions of this invention.
WO2005023225A1 Cilostazol adsorbate The invention relates to cilostazol adsorbates, and processes for their preparation. It also relates to oral pharmaceutical compositions that include the cilostazol adsorbate.
WO2008087862A1 Agent against periodontal disease It is intended to provide a drug or a food or a drink which contains a highly safe compound originating in a natural material as the active ingredient, promotes the blood flow in the periodontal tissue and induces basic fibroblast growth factor in the periodontal tissue or the alveolar bone to thereby exert the function of regenerating the periodontal tissue or the alveolar bone having been broken or reduced by periodontal disease. A drug or a food or a drink which contains, as the active ingredient, an adenine-based nucleic acid compound such as adenosine or AMP is provided. The above-described drug, food or drink promotes the blood flow topically in the periodontal tissue, and induces and produces basic fibroblast growth factor that is capable of strongly inducing the regeneration of the tissue per se. Thus, the drug, food or drink can artificially induce and promote the regeneration of the periodontal tissue having been lost as the periodontal disease proceeds, which makes it usable as a preventive or a remedy for periodontal disease.
WO2008027854A3 Pharmaceutical compositions comprising hgh for oral delivery The present invention relates to dosage forms of human growth hormone, the use of an absorption enhancer to allow absorption of human growth hormone into the systemic circulation in a biologically active form, in particular after oral administration, as well as the use of oral dosage forms comprising human growth hormone and an absorption enhancer for the treatment of human growth hormone deficiencies and disorders associated therewith.
US8735408 Solid forms of 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl dimethylcarbamate Solid forms of 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl dimethylcarbamate and salts thereof are disclosed. Methods of its use to treat diseases and disorders of the eye are also disclosed.
EP0877740B1 Thiol derivatives with metallopeptidase inhibitory activity Compounds of formula (I), wherein R, R1, R2, and R3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
WO2008090940A1 Pharmaceutical agent comprising dopamine d2-like receptor agonist as active ingredient and screening method Disclosed are: a pharmaceutical agent which is effective on a disease induced by the over-response of Th2 or Th17 (e.g., multiple sclerosis); and a method for efficient screening of the pharmaceutical agent. Specifically disclosed are: a pharmaceutical agent for the treatment or prevention of a disease induced by the over-response of Th2 or Th17, which is characterized by comprising a dopamine D2-like receptor agonist as an active ingredient; and a method for screening of the pharmaceutical agent, which is characterized by utilizing the binding to a dopamine D2-like receptor and/or the active effect on a dopamine D2-like receptor as an indicator.
CN101200741A Synthesis of conjugated linoleic acid glyceride derivatives based on enzyme method The invention relates to a conjugated linoleic acid glycerides derivative which mainly includes conjugated linoleic acid signal glyceride, conjugated linoleic acid diglyceride and conjugated linoleic acid polyglycerol ester. The product takes the fat with linoleic acid as raw material. The conjugated linoleic acid with high purity is obtained after the alkali isomerization and the molecular distillation purification. Then, the product is obtained under the normal temperature and the normal pressure after the enzymatic promoted catalytic reaction. Compared with the conjugated linoleic acid, the stability and the taste of the product are greatly improved. The invention can be widely applied to the fields of medicine, nutritional health products, food additives, functional feed additives, etc.
US20120129825 Method for on-demand contraception using levonorgestrel or norgestrel The invention relates to a method for contraception, which method comprises on-demand administering levonorgestrel or norgestrel in a woman, within 24 hours before an intercourse.
US7345050 Imidazo(1,2a)pyridine or pyrazolo(2,3a)pyridine derivatives; Alzheimer's and Parkinson's Disease; nervous system, brain, and psychological disorders The present invention relates to new compounds of the formula (I) a process for their preparation, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, as well as intermediates used in the preparation of said active compounds
US20080125474 Pyrazole Analogs The invention relates to the compounds of formula (I): or a pharmaceutically acceptable salt and solvate thereof, wherein R1 is F or H and to processes for the preparation of, intermediates used in the preparation of, compositions containing the uses of, such compounds. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular allergic and respiratory diseases, disorders and conditions
CN102697802A Composite calcium preparation and preparation method thereof A composite calcium preparation in dosage form of soft capsule comprises (by weight) 51-70 parts of calcium carbonate, 1-10 parts of calcium citrate and 0.0001-0.5 parts of calcium absorption promoter as materials; and 1-5 parts of beeswax and 20-40 parts of vegetable oil as adjuvants. Another composite calcium preparation in dosage form of chewing tablet comprises (by weight) 15-35 parts of calcium carbonate, 3-15 parts of calcium citrate and 20-55 parts of calcium absorption promoter as materials; and 10-40 parts of mannitol, 2-10 parts of milk powder, 0.05-10 parts of hydroxypropyl methylcellulose, 0.01-0.05 parts of trichlorosucrose, 0.01-0.8 parts of malic acid, 0.1-2 parts of silicon dioxide and 0.1-2 parts of magnesium stearate as adjuvants. The composite calcium preparation reduces side effect risk of single calcium source, and improves calcium absorption rate.
US6951868 Central nervous system disorders, gastrointestinal disorders;side effect reduction The invention provides compounds of Formula I: wherein Azabicyclo is any of: These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which α7 is known to be involved.
US20110229587 Calcium Supplements for the Treatment of Diabetes Provided herein is a method for treating diabetes, said method comprising administering to a subject with diabetes a composition comprising calcium.
US20080069825 Multiple CpG oligodeoxynucleotides and their use to induce an immune response Compositions including multiple oligodeoxynucleotides with a CpG motif are disclosed herein. The compositions can include either D or K type oligodeoxynucleotides. These compositions are of use in inducing an immune response in a large percentage of the individuals in a population.
EP1634594A1 Use of 3-substituted oxindole derivatives as KCNQ potassium channel modulators The present invention relates to the use of substituted 3-phenyl oxindole derivatives as modulators of the potassium KCNQ channels, to pharmaceutical compositions comprising these compounds, and to methods of treatment herewith.
CN103432082A Glucosamine composition and preparation method thereof The invention relates to a pharmaceutical composition of glucosamine, and specifically relates to a pellet preparation suitable for oral administration and prepared from glucosamine or a pharmaceutically acceptable salt of the glucosamine, and a preparation method thereof. The glucosamine pellets contain the glucosamine or the pharmaceutically acceptable salt of the glucosamine, a diluent, a disintegrating agent, a binder and other pharmaceutic adjuvants; the grain size of the pellets is generally in the range from 0.1 to 10 mm, preferably from 0.1 to 5 mm and more preferably from 0.1 to 2 mm. The glucosamine pellets provided by the invention can be directly filled into capsules or pressed into tablets; as the pellet process is adopted, the wet granulation process of a common preparation is simplified, the probability of the glucosamine being wet is reduced and the stability of the product is improved; the glucosamine pellets are convenient to take, especially for gastric ulcer sufferers.
US7087223 Preventives and/or remedies for hyperphosphatemia Provided in a phosphate ion adsorbent containing a weakly basic anion exchange resin as an active ingredient which aims at providing preventives and/or remedies for hyperphosphatemia having a high selectivity for the adsorption of phosphate ion and showing an effect of lowering blood phosphorus level and another effect of suppressing phosphorus excretion into the urine.
US20090005354 New Amino Derivatives and Their Use as Pharmaceuticals The present invention provides for compounds of formula (I): which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.
CN101596193B Application of palmatine in medicine for treating yellow fever virus infection The invention discloses an application of palmatine for preparing medicine for treating and preventing yellow fever virus infection; the inhibition ratio of palmatine to yellow fever virus (YFV) under the condition that the concentration of the palmatine is 100mu m is 96.58 percent, and the survival rate of Vero cells is 92.93 percent under the condition that the concentration of the palmatine is100mu m. The palmatine can effectively inhibit proliferation of yellow fever virus, but has low cytotoxicity, therefore, the palmatine can be further developed into the medicine for treating diseasescaused by yellow fever virus infection and has wide application prospect.
EP1603544A1 Treatment of intestinal conditions with n-2,3,3-tetramethylbicyclo 2.2.1 heptan-2-amine The present invention is directed to methods and formulations for reducing, preventing, and/or managing abnormal increases in gastrointestinal motility, and intestinal conditions that cause the same. Methods of using N-2,2,3-tetramethylbicyclo-[2.1.1]heptane-2-amine and formulations comprising N-2,2,3-tetramethylbicyclo-[2.1.1]heptan-2-amine are included.
WO2013043985A1 Edible oils to enhance delivery of orally administered steroids The present invention relates to the formulation of steroids, including neurosteroids (e.g., allopregnanolone (ALP)) in edible oils to enhance their absorption when administered, e.g., orally or transmucosally to a patient.
WO2006050826A2 Treatment of mastitis with enrofloxacin The invention relates to the simplified treatment of mastitis, with enrofloxacin or ciprofloxacin, in particular, in cattle.
CN1569023A Chitosan chewing tablet and its preparation method Disclosed is chitosan chewing tablet and its preparation method, wherein the tablet comprises chitosan and pre-gelatinated modified starch, whose weight proportion is 10-30 parts and 20-40 parts.
WO2009023752A1 Adrenergic compounds Disclosed herein is an alpha - adrenergic compound having a structure. Therapeutic methods, compositions, and medicaments for treating pain are also disclosed herein.
CN1723905A Cefdinir oral disintegration tablet, and its prepn. method An oral disintegrating tablet of Toubaodini is prepared from Toubaodini, filler, disintegration agent, flouring agent, sweeten and appropriate. It features that it can be easily dissolved in saliva.
US20110319365 Complexes of 4-hydroperoxy ifosfamide as anti-tumor agents The present disclosure concerns complexes of 4-hydroperoxy ifosfamide. In one embodiment the complexes can be represented by the formula wherein A represents an ammonium species selected from the conjugate acid of a basic amino acid, quaternary ammonium, aliphatic ammonium, heterocyclic ammonium, aromatic ammonium, substituted and unsubstituted pyridinium, guanidinium, and amidinium, and wherein X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.
WO2007074171A1 Aza heterocyclics for the treatment of malaria or aids Methods for the synthesis of various novel substituted dipeptide derived nitrogen-containing heterocyclic compounds (I) and their pharmaceutically acceptable salt derivatives are provided. The compounds of the invention are claimed and are useful as medicaments for the treatment or prevention of disease in a mammal, for example a human. In particular the compounds are useful as immuno therapeutics and anti -microbial drugs or vaccines. These heterocyclic derivatives can be used as an active agent in a pharmaceutical, as well as a diagnostic utility.
CN1927196A Preparing process for freeze-dried calcium gluconate powder injection The invention discloses a calcium gluconate lyophilized preparation for injection and its technical preparation, the main constituent of which is calcium gluconate, its process steps are as follows : calcium gluconate raw material, plus aqua pro injectione is boiled and disslolved, coarse filtered, remove the heat source by adding activated carbon, filtrate with aseptic filteration, sterile-packed in sterile glass bottles, freezed in freeze dryer, dried and molded, hermetization block, stamped cover and pricked with aluminium cover, packed and warehoused.
CA2381354C Utilisation de la cyamemazine dans le traitement du sevrage brutal aux benzodiazepines The invention concerns the use of cyamemazine or its pharmaceutically acceptable salts for cold turkey treatment with benzodiazepines.
US20140178369 Treatment with anti-vegf antibodies This invention concerns in general treatment of diseases and pathological conditions with anti-VEGF antibodies. More specifically, the invention concerns the treatment of human patients susceptible to or diagnosed with cancer using an anti-VEGF antibody, preferably in combination with one or more additional anti-tumor therapeutic agents.
WO2012097039A1 Imidazo [4, 5 -c] quinolin- 2 -one compound and its use as pi3 kinase / mtor dual inhibitor The present invention provides an imidazo[4,5-c]quinolin-2-one compound (formula (I)), or a pharmaceutically acceptable salt thereof, that inhibits both PI3K and mTOR and, therefore, is useful in the treatment of cancer.
EP1690544A2 Pharmaceutical composition containing decoy and method of using the same A pharmaceutical composition for performing treatment against a skin disease, the pharmaceutical composition comprising at least one decoy and a pharmaceutically acceptable carrier. The at least one decoy may be selected from the group consisting of an NF-κB decoy, a STAT-1 decoy, a GATA-3 decoy, a STAT-6 decoy, an AP-1 decoy and an Ets decoy. The at least one decoy may be an oligonucleotide including at least two decoys bonded to each other, the at least two decoys being selected from the group consisting of an NF-κB decoy, a STAT-1 decoy, a GATA-3 decoy, a STAT-6 decoy, an AP-1 decoy and an Ets decoy. The skin disease may be atopic dermatitis, psoriasis vulgaris, contact dermatitis, keloid, bedsore, ulcerative colitis, orCrohn's disease.
EP2220057A2 Prostaglandin e1 and e2 analogs for the treatment of various medical conditions A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.
WO2002028345A3 Aldehyde-releasing compounds A method of treating cancer, comprising the step of administering to a subject in need thereof an effective amount of a compound or compounds which increase or supplement the intracellular levels of endogenous aldehyde, prior to, together with, or subsequent to the administration of a therapeutically-effective amount of a chemotherapeutic agent such as anthracyclines and anthracenediones, wherein the efficacy of the chemotherapeutic agent is enhanced relative to the efficacy of the chemotherapeutic agent alone. The compound may be an aldehyde-releasing compound (preferably formaldehyde), including known aldehyde-releasing compounds and two new classes of aldehyde-releasing compounds. One new class of aldehyde-releasing compounds of formula (II) release more than one equivalent of aldehyde Z-(L-M?1-CHR-M2)¿x (II) wherein x is an integer of 2 or more Z is a direct bond or a linking group of valency x; L is either a direct bond or a spacer group R is H or C1-4 alkyl, alkenyl or alkynyl; M1 is a decomposable or hydrolysable group; and M2 is a second decomposable or hydrolysable group. Another new class of aldehyde-releasing compounds include a radical based on an inhibitor of an aldehyde detoxifying agent, such as buthionine sulphoximine or crotonaldehyde.
EP1863464B1 O-desmethylvenlafaxine and bazedoxifene combination product and uses thereof A combination product containing at least two active compounds, O- desmethylvenlafaxine or a pharmaceutically acceptable salt thereof and bazedoxifene or a pharmaceutically acceptable salt thereof is described. Also described are methods of making and using this combination product to treat a variety of conditions associated with low circulating estrogen levels or low estrogen receptor activity.
CN102370947A External preparation with effects of diminishing inflammation, relieving itching, disinfecting and sterilizing and preparation method thereof The invention belongs to the field of medicine and particularly relates to an external preparation with the effects of diminishing inflammation, relieving itching, disinfecting and sterilizing and a preparation method thereof. The invention needs to solve the technical problems of carrying out improvement aiming at a Binghuangfule ointment and enhancing the curative effect and the compliance of a patient. The external preparation comprises the following bulk drugs proportioned by weight: 20 to 68 parts of rhubarb, 1 to 40 parts of turmeric, 1 to 10 parts of baikal skullcap root, 3 to 10 parts of licorice, 20 to 40 parts of sulfur, 0.1 to 6.5 parts of borneol and 0.1 to 4.5 parts of menthol; and the improvement is characterized in the extraction method of the bulk drugs. The preparation method of the external preparation comprises the following steps: (A) extracting the rhubarb, the turmeric, the baikal skullcap root and the licorice by using water or alcohol so as to obtain an extract for standby application; and (B) preparing the external preparation by the extract, the sulfur, the borneol, the menthol and acceptable auxiliary materials in pharmacy according to a conventional method in the pharmacy. The preparation process of the external preparation disclosed by the invention is simple and convenient, the operation is easy, and the external preparation obtained by preparation has an obvious curative effect in clinic and is better than an ointment; and moreover, the external preparation does not taint clothing, and the compliance of the patient is good.
CN102603719A Novel compound of 2-furylcarbinol-(5'-11)-1,3-cyclopentadiene [5,4-c]-1H-cinnoline and application of novel compound as antioxidant to food, cosmetics or medicine The invention provides a novel compound of 2-furylcarbinol-(5'-11)-1,3-cyclopentadiene [5,4-c]-1H-cinnoline, which has a molecular formula of C16H12N2O2. A preparation method comprises the steps that: Cichorium endivia L. is cultured, and dried herb is subjected to ethanol collection, sherwood oil and ethyl acetate extraction, 60-percent ethanol eluting in macroporous resin, n-butyl alcohol and 5-percent NaHCO3 extraction and repeatedly eluted by methanol water solution in preparation of reverse phase-high performance liquid chromatography (RP-HPLC). The compound provided by the invention has good antioxidation activity and can be used as an antioxidant to be applied to food, cosmetics and medicine.
EP2648727A2 Compositions and methods for mobilizing stem cells The present invention relates to the field of hematopoietic stem cells. More specifically, the present invention provides methods and composition useful for peripheral blood stem cell mobilization. In one embodiment, a method of treating an organ transplant recipient comprises administering to the recipient a low dose of Tacrolimus in an amount sufficient to mobilize stem cells to the peripheral blood of the recipient. In a specific embodiment, the low dose of Tacrolimus is in the range of about 0.05 mg/kg to about 0.5 mg/kg.
WO2012167281A2 Clinical application utilizing genetic data for effective medication management The present disclosure relates a predictive method, based on a subject's genetic profile, which defines variability in a specific disease or condition to determine medication response, including determining select VNTR and SNP occurrence combinations which are associated with specific responses to medications, kits and DNA chips/arrays containing such combinations so as to effectuate better medication management.
WO2007112098A2 Uses of diphenyl/diphenylamine carboxylic acids The present invention demonstrates that chemical-induced degradation of Sp proteins by a specific sub-class of NSAIDs inhibited cancer cell growth, angiogenesis and metastasis of cancer cells. The inhibitory effects of these compounds were demonstrated in vitro and in vivo. Hence, the results discussed herein indicate that these compounds can be used to inhibit cell growth, angiogenesis and metastasis in cancers such as pancreatic, breast, prostate, colon, bladder and ovarian cancers.
EP1385510A4 Prodigiosin composition for the treatment of rheumatic arthritis The present invention relates to novel use of prodigiosin for the treatment of Rheumatic arthritis and can provide excellent treatment effect to Rheumatic arthritis by treating composition including prodigiosin isolated from Serratia marcescence as an active principle to DBA-1 mouse of collagen-induced Rheumatic arthritis animal model and thereby inhibiting production of internal cytokine which is a important pathogen of Rheumatic arthritis.
CN1795867A Liposome of doxorubicin and prepration method and application A doxorubicin-lipid composition for treating the pancreas cancer of mammal and its preparing process are disclosed.
US20070298058 Pharmaceutical compositions comprising ascomycin The invention relates to pharmaceutical compositions comprising an ascomycin in dissolved form and a pharmaceutically acceptable cellulose derivative for prevention or reduction of crystal growth.
WO2008032054A2 Composite material comprising a tissue matrix compound and a bioactive glass The present invention provides a composite material comprising a tissue matrix compound and a bioactive glass. The invention also relates to pharmaceutical and cosmetic compositions containing the composite material. Further aspects of the invention relate to the use of the composite material for treating a skin blemish or augmenting soft tissue.
CN101194897A Method for preparing water-solubility compound vitamin microcapsule The invention relates to a process for preparation of a water-soluble complex vitamin capsule. In order to solve the problems that some water-soluble vitamins are not stable or have imperfect odor, the invention takes five mixtures of vitamins which comprise thiamine hydrochloride (namely vitamin B1), riboflavin (namely vitamin B2), pyridoxine hydrochloride (namely vitamin B6), folic acid and niacinamide as core material, and the invention takes xanthan gum or acacia gum or guar gum or gelatin as wall material to prepare water-soluble complex vitamin capsule. The key point of the process for preparation is that respectively preparing wall material water solution and core material water solution, and then evenly mixing the wall material water solution and the core material water solution to get mixture, and water-soluble complex vitamin capsule products with excellent sensory characteristics can be prepared after the mixture which is got is pre-frozen, frozen and dried, disintegrated, and screened in turn. The products have excellent heat stability and light stability, which can be used as special-purpose type food batching to apply in food processing, and can be used to strengthen water-soluble vitamin in food.
US8828446 Method for reducing transplant rejection in the eye and intraocular implants for use therefor Methods for reducing or preventing transplant rejection in the eye of an individual are described, comprising: a) performing an ocular transplant procedure; and b) implanting in the eye a bioerodible drug delivery system comprising an immunosuppressive agent and a bioerodible polymer.
CN101375836A Compound gentamicin-micronomicin injection and preparation method The invention provides a compound gentamycin-micronomicin injection which causes the causative organisms to be not easy to generate drug resistance and a preparation method thereof. The injection comprises 80 to 110 parts of compound gentamycin-micronomicin, 60 to 150 parts of aminopyrine, 5 to 20 parts of bethanechol chloride, 2 to 20 parts of dexamethasone sodium phosphate, and 100 to 400 parts of 95-percent ethanol. The preparation method comprises the following steps: aminopyrine is put into 95-percent ethanol, and is stirred for 10 to 25 minutes to become transparent; 300 parts of water for injecting is taken, gentamycin-micronomicin, bethanechol chloride, dexamethasone sodium phosphate are added in sequence to water, and stirred until being dissolved, and the liquid is mixed; the injection is stirred evenly, and kept for 15 to 20 minutes; when the liquid medicine becomes transparent, 1000 parts of water for injection is added, so that the injection is obtained. By adopting a polypharmacy pharmaceutical, the injection is effective for bacterial stomach intestine of a pig, a cow, a sheep and a horse, the resistance of an organism is enhanced, both the symptoms and the root causes are addressed, and the stress reaction of an animal body is eased.
EP1712235A2 Combinational therapy involving a small molecule inhibitor of the MDM2: P53 interaction The present invention is directed to a combinational therapy for treating cancer or other cell proliferative diseases. Such a therapy combines the use of radiation therapy or chemotherapy with the use of a small molecule inhibitor of the MDM2: p53 interaction.
EP1427739A4 Targeted bisplatinum polyamines as pro-drugs: selective release of platinum Pro-drug forms of linear polyamine-bridged platinum compounds and methods for their production and use are provided. The polyamine-bridge portion of the compounds is based on spermine or spermidine, and the central amines of the polyamine-bridge are chemically bonded to labile blocking groups. The presence of the blocking groups serves to minimize the toxicity of the Pt compounds upon administration. Selective removal of the blocking groups and release of the active, unblocked species occurs upon exposure to suitable environmental conditions.
US20090181943 Inhibitors of Histone Deacetylase This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.
EP1637156A1 Systemic administration of osteogenic proteins in the treatment of metabolic bone diseases The invention is a treatment for increasing the bone mass or preventing bone loss in an individual afflicted with a bone disease which includes administering to the individual a morphogen in a therapeutically effective amount so as to maintain or stimulate bone formation.
EP0861247B1 Novel imidazole n-benzyldioxol derivatives, method for preparing same, resulting intermediates, pharmaceutical compositions and use of said derivatives as endothelin antagonists Novel compounds of formula (I), wherein R1 is optionally substituted alkyl or cycloalkyl optionally interrupted by heteroatoms, both of R2 and R3 are or carry an acid isostere or acid function, and Y is phenyl particularly substituted by a dioxol radical, said compounds being in all isomeric and salt forms, for use as drugs.
US20050119159 Remedy for ischemic heart failure In the process of extensively searching for a drug elevating the survival ratio in ischemic heart failure, in particular postinfarction heart failure, it is found out that βARKct which is a βARK1 inhibitor is efficacious not only in improving heart function but also elevating survival ratio in postinfarction heart failure. Accordingly, it is expected that the βARK1 inhibitor is efficaciously usable as a remedy for ischemic heart failure which exerts not only an effect of improving heart function but also another effect of elevating survival ratio and, in its turn, contributes to the improved prognosis in patients with ischemic heart diseases.
US20050209252 Using an indazole compound This invention relates to a method for treating cancer including administrating to a subject in need thereof an effective amount of a compound of the formula: wherein, A is H or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH═NOR, (CH2)mC(O)N(OR)R′, N(OR)R′, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.
CN102335146A Injectable drug combination and preparation method thereof The invention provides an injectable drug combination and a preparation method thereof. The injection preparation which is a freeze-dried powder injection comprises salvianolic acid B and a pharmacologically allowable pH regulator, without other excipients. The addition of the pH regulator is pH being 4-5 in the pre-freeze drying system. The salvianolic acid B injection preparation provided by the invention selects a proper pH range without the addition of a supporting agent to ensure the stabilization of the injection as well as the pharmacological acceptability of the injection. The invention has advantages of safe clinical use, no bad effect of inducing hemolysis, good safety and stable quality for long-term storage with the stability and safety completely meeting the requirement of the injection preparation and the requirement of clinical application. The injection prepared by the technology needs no addition of auxiliary materials such as a stabilizer, a freeze-drying excipient and so on and the hidden danger of the injection is decreased. The invention avoids the use of magnesium salt and the side effect of magnesium ion to cardiovascular system can be prevented.
US8461165 2-Substituted phenyl-5,7-dihydrocarbyl-3,7-dihydropyrrolo[2,3-d] pyrimidin-4-one derivatives, the preparation and the pharmaceutical use thereof The invention relates to the compounds of formula I, their preparation and the pharmaceutical compositions containing the compounds. The invention also relates to the use of the compounds of formula I in preparing medicines, which can treat sexual dysfunction of animals including human (male and female), especially erectile dysfunction of male and the diseases in which the function of phospholipase 5 (cGMP PDE5) is involved.
US8048911 Melanin eliminator preparation A melanin eliminator preparation comprising a metal chelate compound represented by the following formula (I), wherein M denotes a metal, and R denotes hydroxyl, O-lower alkyl, an amine bonded at N, an amino acid bonded at N, or a peptide bonded at N, or a pharmacologically acceptable salt thereof.
US20070212325 Insulin Resistance-Improving Agent A medicament comprising a pharmaceutically acceptable anion exchange resin as an active ingredient is provided which exhibits an insulin resistance-improving action regardless of volume of meal or glucose absorption from the gastrointestinal tract.
US20100209542 Methods For Treating Withdrawal From Addictive Compounds Kratom (Mitragynia speciosa korth) is recognized increasingly as a remedy for opioid withdrawal by individuals who self-treat chronic pain and/or generalized substance abuse. For example, opioid withdrawal from an abrupt cessation of opiate abuse may be self-managed by using Kratom. Further, high-throughput molecular screening identified that a major component of Kratom (i.e., for example, mitragyinine) displayed high binding affinity at mu, delta and kappa opiate receptors. The present invention contemplates that Kratom extract may also be useful for the treatment of other addictive drugs besides opiate derivatives.
CN102166215A Pharmaceutical composition containing piperazine derivatives The invention relates to a pharmaceutical composition which contains piperazine derivatives shown in the formula (1) and at least one cardiovascular and cerebrovascular medicament as well as pharmaceutically acceptable carrier, and also relates to a medical box containing the active matters. The composition or the medical box is used for preventing, delaying or treating the following diseases or symptoms of patients: type II diabetes, diabetic complications, hyperglycemia, obesity, insulin resistance, hypertension, hypertension complications, dyslipidemia, coronary heart disease, angina, congestive heart failure, arrhythmia, cerebral apoplexy, arteriosclerosis, cerebral infarction, ischemic diseases, cerebrovascular diseases, cardiovascular diseases, coronary artery diseases, sexual dysfunction, cognitive dysfunction, ventricular dysfunction, cardiac insufficiency, pulmonary vascular diseases or renal vascular diseases. The pharmaceutical composition provided by the invention lowers the morbidity rate and/or mortality rate of cardiovascular and cerebrovascular diseases, reduces the adverse reaction and simultaneously improves the medicament taking compliance of patients.
EP1377575B1 Antiviral pyrazolopyridine compounds The present invention provides compounds of formula (I), pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. The compounds are useful in the prophylaxis treatment of herpes viral infections.
CN1580054A Pentatomic sulphur heterocyclic compound and its use for preparing medicine for treating preventing diseases related to adiposity The invention refers to the anti form of the general equation I, quinary sulfureous heterocyclic compound and its despinners or optical isomer or its medical salt or hydrate or pharmic combination with refered compound and the definitions of all the substituent are explained in the right-claiming document. The invention also refers to the preparation method of the compound in the general equation I and their uses in producing weight reducing medicines and antineoplastic medicines.
CN1957927A Fat micro sphere preparation of triterpenoid saponin and derivative, and fabricating method A lipid microball of triterpenoid saponin or its derivative is prepared from triterpenoid saponin or its derivative and the pharmacologically acceptable edible oil for injection, emulsifier, emulsifying aid, stabilizer, isotonic agent, antioxidant and the water for injection. Its preparing process is also disclosed.
WO2006093034A1 Mental disorder-related gene and use of the same Disclosed is useful means for the therapy or diagnosis of a mental disorder. A method for screening for a compound which is effective for a mental disorder, comprising the steps of (1) providing a cell capable of expressing a gene (target gene) selected from the group consisting of a gene having the nucleotide sequence depicted in SEQ ID NO:1, a gene having the nucleotide sequence depicted in SEQ ID NO:2, a gene having the nucleotide sequence depicted in SEQ ID NO:3 and genes homologous to these genes; (2) exposing the cell to a compound to be tested; (3) determining the amount of a product of the target gene expressed in the cell after the exposure to the compound; and (4) determining the change in amount of the product of the target gene under the influence of exposure to the compound.
WO2009041559A1 Indazole acrylic acid amide compound Disclosed is a compound represented by the formula shown below and a pharmaceutically acceptable salt thereof, which is useful as an IKur-blocker that is useful for the prevention or treatment of cardiac arrhythmia such as atrial fibrillation. wherein the ring X represents a benzene or a pyridine; R1 represents a substituted alkyl; R2 represents an aryl which may be substituted or a heterocyclic group which may be substituted; R3 represents a hydrogen or an alkyl; R4 represents a hydrogen, a halogen or an alkyl; R5 represents a hydrogen or an alkyl; and R6 and R7 independently represent a hydrogen or a halogen.
WO2010109421A1 A medicinal antifungal and steroids cream comprising chitosan and a process to make it The present invention relates to a composition for treating fungal skin infections particularly dandruff, along with skin/scalp rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, and an antifungal/antidandruff active ingredient. It discloses a composition for treating fungal skin infections particularly dandruff, along with skin/scalp rejuvenation containing a) a biopolymer in the form of Chitosan, b) an active pharmaceutical ingredient (API) alone or in combination used in treating fungal skin infections particularly dandruff related, c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants, and d) water. The active ingredients, namely chitosan, and an anti fungal / antidandruff agent, are incorporated in cream base for use in treating fungal infections and dandruff.
CA2714478A1 Dental sterilizing water, method for producing the water, and device for producing the water This aims to produce dental sterilizing water having not only a sterilizing action but also an action to break a bio-film. Provided is a sterilizing water producing device (51) comprising a stock solution tank (3) for storing a stock solution (52), a stroke pump (4) connected in communication to the stock solution tank, an electrolytic bath (5) connected in communication to the stroke pump, a discharge pipe (6) connected in communication to the electrolytic bath, and a dilution water tank (8) reserving dilution water (57). The dilution water tank (8) is so positioned relative to the tip position of the discharge pipe (6) that the tip of the discharge pipe (6) may be lower than the water level of the dilution water (57) reserved in the dilution water tank (8). The stock solution (52) is prepared by selecting any of the methods shown at (a-1) to (d).
CN1954815A Anti-tuberculosis compound medicine quick-slow double-release preparation and its preparation method A both fast-release and slow-release compound medicine for preventing and treating tuberculosis (TB) is prepared from rifampin and isoniazid. Its preparing process is also disclosed.
US8088760 Benzoxazole carboxamide inhibitors of poly(ADP-ribose)polymerase (PARP) A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
DE102007022448A1 Cosmetic or dermatological skin treatment agent, useful as skin brightening active agent and for non-therapeutic, cosmetic treatment of the skin, comprises photocatalytically active metal oxide in a carrier Cosmetic or dermatological skin treatment agent (I) comprises at least a photocatalytically active metal oxide as skin brightening active agent, in a carrier. An independent claim is included for a method for non-therapeutic, cosmetic treatment of the skin comprising applying (I) on the skin, preferably face skin, skin of the cleavage, back stretch and/or on age spots, freckle and/or birth mark, and exposing the applied body surface to light at 300-1200, preferably 380-800 nm.
EP2292629A1 Method of isolating cytisine from biomaterial The present invention concerns a method for extracting cytisine from biomaterial wherein the biomaterial is contacted with an alkaline aqueous solution, but in the absence of any other co-solvent such as an organic phase. Cytisine is recovered from the alkaline aqueous extract by extraction of the extract with rapeseed oil which in turn is extracted with an acidic aqueous phase.
WO2009017755A3 Cb1 antagonists and inverse agonists The present invention relates to methods of treating obesity, anorexia nervosa, or bulimia nervosa comprising administering a compound of the invention conjointly with zonisamide, naltrexone, or a pharmaceutically acceptable salt thereof. The present invention further relates to the treatment of metabolic syndrome comprising administering a compound of the invention conjointly with zonisamide, naltrexone, or a pharmaceutically acceptable salt thereof.
US20090209615 Inhibitors of matrix metalloproteinases to treat neurological disorders The invention provides methods to treat neurological disorders, opthalmological disorders, or a combination thereof by administering a compound that inhibits MMPs. A compound that inhibits MMPs is represented by the compound of formula (I) shown herein.
WO2009058076A1 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase The invention provides compounds of formula (I) wherein R1, R3, R4, R5, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.
CN1891303A Method for preparing bile acid adsorbent of beta cyclo dextrin polymer This invention discloses a preparation method for bile acid sorbent of beta-ring dextrin polymer including: mixing beta-ring dextrin with crosslinking agent epoxy chloropropane, 1, 2 glycop twice-shrunk glyceryl ether or 1, 2-butylene-glycol twice-shrunk glyceryl ether, then dropping 37% thick HCL, 98% thick HNO3, 98% H2SO4 or perchloric acid in it to be mixed to get the bile acid sorbent of beta-ring dextrin polymer, or firstly solving the epoxy chloropropane, the 1,2-glycop twice-shrunk glyceryl ether or 1,2-butylene-glycol twi-shrunk glyceryl ether in tetrachloroethylene then solving the beta-ring dextrin solution in the tetrachloroethylene solution, then adding 37% thick HCL, 98% H2SO4 or perchloric acid in it to be reacted to get the sorbent.
CN101385824A Medicine for treating glaucoma, cataract, pinkeye and near sightedness and preparation method thereof The invention discloses a drug for treating glaucoma, cataract, pinkeye and myopia. The drug is made from Chinese date and dried old orange peel based on a certain weight proportion. The drug has the functions of detoxification, promoting the production of body fluid, dredging capillary vessels and regulating optic nerve, and is used for treating various eye diseases such as the glaucoma, the cataract, the pinkeye, the myopia, keratitis, retinal detachment, blurred vision and the like. The drug has good effect and high curative rate.
CN102796083A Spiro heterocyclic ketone N-phenyl indole compound, its preparation method and application in controlling cardiovascular diseases and other medicine fields The invention discloses a spiro heterocyclic ketone N-phenyl indole compound, its preparation method and application in controlling cardiovascular diseases and other medicine fields. The compound is formed by organically connecting spiro heterocycle, indole, phenyl ring and tetrazole, is an AT1 type acceptor retarding agent of angiotensin II, and can be used for preventing or treating hypertension, coronary heart disease, disease in blood vessels of heart, brain and kidney, hemicrania, pulmonary hypertension and other diseases.
US20090042854 Hexahydro-3H-Pyrrolizin-3-Ones Useful as Tachykinin Receptor Antagonists The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
CA2343325C Topical dermal antimicrobial compositions The present invention relates to a topical antimicrobial composition containing an antimicrobial complex that provides sustained antimicrobial disinfecting action upon contact with microorganisms for prolonged periods, without the necessity for reapplication. The topical antimicrobial composition provides both initial and residual contact-killing disinfecting activity, and does not release its antimicrobial components into contacting liquids at levels that result in solution disinfection.
US20110183011 Composition and method for topical treatment of skin lesions Disclosed herein is a composition containing a high concentration of PG is unexpectedly capable of quickly killing other bacteria, fungi, and/or virus in vitro that is indicative of its potential high efficacy in treating various skin infection. Embodiments disclosed herein relate to a composition and method for effective topical treatment of inflammatory skin lesions in mammals, comprising of a high concentration of propylene glycol alone, or in combination with an astringent. The PG at high concentrations can be regarded as an extremely effective, safe, topical, universal, microbicide.
US20110117055 Methods of Treating Hepatitis C Virus with Oxoacetamide Compounds Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.
CN1843341A Use of rhubarb anthraquinone compound in preventing and treating influenza virus infectious disease The invention relates to an application of anthraquinones compound in preventing diseases infected by influenza virus. The median poison concentration TC50 of anthraquinones compound for cell MDCK is 226.1 ug/ml, the comparison is 351.3 ug/ml; the median effective concentration LC50 for influenza virus is122.4 ug/ml, the comparison is 62.7 ug/ml; and the treating index is 1.9. It is proved that the inhibiting rate for influenza virus is increased with increased drug concentration. The side effect of nthraquinones compound is smaller than that of ribavirin, the process is simple and it can be prepared into various dosage forms.
EP2611804A1 Novel compounds and compositions for the inhibition of nampt The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:
US20070259879 Piperazine and piperidine biaryl derivatives This invention relates to piperazine and piperidine biaryl compounds of Formula (I): or a pharmaceutically acceptable prodrug, salt, polymorph, solvate, enantiomer, diastereomer, racemate, mixture of stereoisomers thereof, or derivative thereof; and to processes for preparing the compounds or pharmaceutical compositions containing the same. The compounds and pharmaceutical compositions of the present invention are provided for use in the treatment of HIV infection and/or AIDS.
WO2012074785A1 Pharmaceutical compositions comprising 3,4- dihydroisoquinolin-2(1 h)-yl-3-phenylurea derivatives having formyl peptide receptor like-1 (fprl-1) agonist or antagonist activity The present invention relates to a method of treating a disorder associated with modulation of the FPRL-1 receptor which comprises administering a therapeutically effective amount of a pharmaceutical composition comprising a 3,4-dihydroisoquinolin-2(1H)-yl-3-phenylurea derivative.
US20050059626 Methods of preventing and treating viral infections using immunomodulatory polynucleotide sequences The invention provides methods of suppression, prevention, and/or treatment of infection by viruses. A polynucleotide comprising an immunostimulatory sequence (an “ISS”) is administered to an individual who is at risk of being exposed to, has been exposed to or is infected with a virus. The ISS-containing polnucleotide is administered without any antigens of the virus. Administration of the ISS-containing polynucleotide results in reduced incidence and/or severity of one or more symptoms of virus infection.
US20080139538 Tertiary Carbinamines Having Substituted Heterocycles Which Are Active As Beta-Secretase Inhibitors For The Treatment Of Alzheimer's Disease The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
WO2011158334A1 Food and orally-administered agent for skin whitening containing zederone or zederone analogue as active ingredient Provided is an orally-administered agent for skin whitening which is easily ingested and highly effective as a skin whitener. Specifically, provided is an orally-administered agent for skin whitening that contains, as an active ingredient, a group of substances and hydrogenated substances that have a specific germacrone-like skeleton and are refined from one or more types of Curcuma zedoaria Roscoe extract. The orally administered agent contains, as active ingredients, zederone, furanodienone, curzerenone, hydrogenated zederone and hydrogenated furanodienone, which are prepared from a Curcuma zedoaria Roscoe extract and are not bitter.
CN102516066A Ostopanic acid, ostopanic acid analogues and their preparation method and use The invention relates to ostopanic acid, ostopanic acid analogues and their preparation method and use. The preparation method provided by the invention is characterized in that based on a characteristic that the reaction of a Weinreb amide and a Grignard reagent can selectively stay in a ketone stage so that the overreaction is avoided, two side chains of the ostopanic acid analogue can be constructed and thus a series of the ostopanic acid analogues can be synthesized fast. The preparation method provided by the invention adopts easily acquired raw materials, allows mild reaction conditions and has simple processes. The ostopanic acid and the ostopanic acid analogues obtained by the preparation method have obvious antitumor effects.
WO2009013343A1 Cosmetic and/or pharmaceutical compositions having antimicrobial activity for topical use, process for the production thereof and the use thereof in the treatment of diseases To produce a cosmetic or pharmaceutical composition having antimicrobial activity, initially silver orthophosphate is generated in photostable form and is then incorporated into a composition for topical use.
CN101933986A Pressure sore paste, preparation method thereof and application thereof The invention relates to pressure sore paste, a preparation method thereof and application thereof. The pressure sore paste comprises the following raw material medicines in part by weight: 80 to 120 parts of oriental buckthorn root, 80 to 120 parts of danshen root, 30 to 60 parts of dog oil and 15 to 20 parts of compound sulfamethoxazole tablets. The preparation method for the pressure sore paste is characterized by comprising the following steps of: (1) slicing the oriental buckthorn root and adding into water with the danshen root, and boiling to obtain liquid medicine; (2) filtering and drying the medicine dregs, grinding into fine powder and adding into the liquid medicine; and (3) adding the dog oil into the liquid medicine, stirring uniformly and boiling to obtain viscous liquid for preparing a medicament for treating pressure sore. The pressure sore paste and the preparation method have the advantages that: the pressure sore paste has functions of relieving pain, activating blood, dissolving stasis, eliminating necrosis and generating muscles, can effectively prevent and treat pressure sore, has obvious curative effect, good curative effect on radiodermatitis and can relieve the pain in patients and improve the living quality of the patients; moreover, a few kinds of raw materials, which are cheap and readily available, are used and the preparation method is simple and easy.
US20110306632 Solid Dispersions Containing Kinase Inhibitors A solid dispersion comprises, in essentially non-crystalline form, a kinase inhibitory compound, e.g., N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a cancer.
US20100298355 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.
US7429612 Indoline compound and medicinal use thereof The present invention provides an indoline compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing this indoline compound or a pharmaceutically acceptable salt thereof. The compound of the present invention shows superior ACAT inhibitory effect and superior lipoperoxidation inhibitory effect and is useful as an ACAT inhibitor or a lipoperoxidation inhibitor.
CN101019950B Qingkailing Preparation for great transfusion and its preparation process The Qingkailing preparation for great transfusion is prepared with cholic acid 1.2-2.0 weight portions, hyodeoxycholic acid 1.4-2.4 weight portions, buffalo horn 9-16 weight portions, baicalin 1.8-3.2 weight portions, nacre 18-32 weight portions, prepared cape jasmine extract liquid 9-16 weight portions, prepared isatis root extract liquid 75-125 weight portions, and prepared honeysuckle extract liquid 23-38 weight portions. The present invention also discloses the preparation process of the Qingkailing preparation for great transfusion. The Qingkailing preparation for great transfusion has high clarity, high stability, high safety and other advantages.
CN101062043A Application of 3, 4, 5, 4'-tetramethyl diphenylethane-3'-O-disodium phosphate in the anti-cancer medicine and the transferring medicine thereof The invention discloses an application of 3, 4, 5, 4'-tetramethoxyl di-ethylbenzene-3' 0-disodium phosphate salt to prepare antineoplastic and inhibit tumor metastasis medicine, which is characterized by the following: inhibiting aggregation of microtubulin; resulting in dysfunction and structural damage of tumour vessel selectively; evoking die of vessel endothelium cell; making the tumor cell lose nourishment and oxygen.
US20120213702 Novel diagnostic agents for the non-invasive in vivo imaging of aminopeptidase n (apn/cd13) The present invention relates to aminopeptidase N (APN) inhibitor conjugates of formula I wherein W is a —CO— or an —SO2— group and at least one of R1 or R2 represents (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and the other represents an alkoxy group or OH, and wherein R3, R3′ and R3″ is independently selected from an alkoxy group or (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and R4 is selected from the group comprising: wherein R is an alkyl group. Furthermore, the present invention relates to a diagnostic and/or pharmaceutical composition comprising the conjugate of the invention. The present invention also relates to the conjugate or composition of the invention for use in the diagnosis or treatment of APN-associated diseases like for example angiogenesis in cancer, rheumatoid arthritis, leukemia and diabetic nephropathy, as well as to the use of the conjugate or of the composition of the invention in the diagnosis or treatment of angiogenesis in cancer, rheumatoid arthritis, leukemia and diabetic nephropathy. In a further aspect, the present invention relates to kits comprising the conjugate or composition of the invention. The conjugate or pharmaceutical/diagnostic composition of the invention can also be used in in vivo or in vitro imaging studies of aminopeptidase N.
CN102743710A Anti-cancer and hemostatic Chinese patent drug The invention discloses anti-cancer and hemostatic Chinese patent drug which comprises the following components by weight: 150 to 200 parts of salsola-like inula flower and herb, 100 parts of white atractylodes rhizome, 100 parts of zedoary, 100 parts of Chinese angelica root, 100 parts of psoralea fruit, 100 parts of pinellia tuber, 100 parts of fritillary bulb, 100 parts of asarum sagittarioides, 60 parts of ginseng, 40 parts of American ginseng, 50 parts of astragalus root, 50 parts of white peony root, 30 parts of rhizome of Sichuan lovage, 50 parts of ass-hide glue, 50 parts of bark of chinese cassia tree, 40 parts of Mabuzi, 7 parts of Banmo, 3 parts of arenobufagin and 40 parts of borneol. The Chinese patent drug has the effects that the curative effect is quick, the Chinese patent drug can effectively restrain complications, is broad-spectrum and anti-cancer, safe, reliable, short in course of treatment, and overcomes the problem of the multidrug resistance of cancer cells, patients can not suffer a relapse after being healed, and the Chinese patent drug has the function of improving the medullary hematopoiesis.
US20130004589 Divalent cation/anion pair containing compositions and methods for treating and/or preventing enzymatic irritation Compositions and methods for treating and/or preventing conditions such as diaper rash and atopic dermatitis are disclosed. The compositions and methods are particularly useful in the treatment and prevention of diaper rash and diaper dermatitis caused by the prolonged contact of human skin with body waste. The methods employ the topical application of a trypsin-inhibiting agent to the area in need of such treatment, or the area where prevention is desired. The trypsin-inhibiting agent is preferably a divalent cation/anion pair.
WO2009107762A1 Aromatic amide derivative Disclosed is a compound represented by general formula (I), which affects the gene transcription process. (I) (In the formula, R1 and R2 each represents a hydrogen atom, an alkyl group, a halogen atom or the like; R3 and R4 each represents a hydrogen atom, an alkyl group, an alkoxy group or an alkenyl group; R5 represents a hydrogen atom, an alkyl group or a nitro group; and R6 represents a hydrogen atom or an alkyl group.)
US20100316697 Methods and compositions for drug targeting The present invention provides methods and compositions for targeting a drug to a specific desired location, such as an intracellular location in a mammalian cell, by causing said drug to migrate along a pH gradient to the specific location, where the drug preferentially accumulates at a pH range of the specific location. Accordingly, the invention described herein is based on providing a drug which is “pH matched” with that of a particular location, such that the drug preferentially migrates to and accumulates at the pH or pH range at that location. The location may be a type of tissue, a type of cell, a sub-cellular location or an intracellular location, such as an organelle. Without being bound to any theory, the drug migrates along or across a pH gradient, and stops migrating and accumulates at a location of specific pH or range of pH at which the drug is energetically neutral, or where its diffusion potential is at a minimum.
US6972297 2-Hydroxy-mutilin carbamate derivatives for antibacterial use 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infections
US20060051754 Transporter selectively transporting sulfate conjugate and its gene It is intended to provide a liver-specific organic anion transporter which transports selectively a sulfate conjugate and its gene. A protein capable of selectively transporting a sulfate conjugate; a gene encoding the same, more specifically, a gene having the amino acid sequence represented by SEQ ID NO:1 in Sequence Listing or the base sequence represented by SEQ ID NO:2; and a method of modifying drug dynamics by altering the ability of a protein to selectively transport a sulfate conjugate with the use of the protein participating in the transport of a sulfate conjugate in the liver, an antibody specific thereto and a substance promoting or inhibiting its function.
EP2404909A1 Amide thiazole derivative, preparation method and uses thereof The present invention relates to the field of the drugs associated with the diabetes. Particularly, the present invention relates to a dipeptidyl peptidase-IV inhibitor having the structure shown by formula (I), which contains amide thiazole structure and has an effect on treating diabetes, and a preparation method and a pharmaceutical composition containing it, as well as use thereof in manufacture of the drugs for treating the diabetes, wherein, R1 is hydrogen, halogen, C1-C5 alkyl, COOR3 or phenyl, wherein R3 is C1-C5 alkyl; R2 is phenyl, substituted phenyl, 2-furanyl, substituted 2-furanyl, 2-thienyl, substituted 2-thienyl, 2-pyrrolyl, or substituted 2-pyrrolyl.
CN1726912A Slow release capsule of compound metformin pyrrolidone and preparation method A slow-releasing capsule of compound fluamine pyrrolinone for treating diabetes is composed of the central slow-releasing fluamine microball or small tablet and the coated fast-releasing pyrrolinone layer. Its advantages are high curative effect and no toxic by-effect.
US20130052231 Treatment methods utilizing stem cell mobilizers and immunosuppressive agents The present invention relates to the field of organ transplantation. In one aspect, the present invention provides methods of treating an organ transplant recipient comprising administering to the recipient a therapeutically effective amount of a stem cell mobilizer and an immunosuppressive agent. In particular embodiments, the present invention provides a method of treating an organ transplant recipient comprising administering to the recipient a therapeutically effective amount of an agent that mobilizes CD34+ and/or CD133+ stem cells and a low dose of an immunosuppressive agent.
CN101928136A Method for preparing fluoridated hydroxyapatite and application thereof The prior art for preparing fluoridated hydroxyapatite needs various compound aqueous solutions and can not prepare fluoridated hydroxyapatite which simultaneously has hydroxyl and a hydroxyl fluorinion hydrogen bond or hydroxyl and different functional group embodiers, such as different hydroxyl fluorinion hydrogen bonds, and the like. Accordingly, the invention aims to prepare fluoridated hydroxyapatite with bioactivity under the condition of changing the calcination temperature and the mixed proportion of calcium fluoride and hydroxyapatite. The fluoridated hydroxyapatite or a composition of the fluoridated hydroxyapatite and other compounds of the invention can be used as skeleton bulking agents and can promote the regeneration and restoration of osteocytes. In addition, the composition of the invention can further contain one or more medical compositions of bone regeneration and restoration so that the medical composition is implanted into animals and plants to further facilitate bone tissue regeneration and restoration in vivo.
WO2007090141A3 Pyrrolo [2, 3, b] pyridine derivatives useful as raf kinase inhibitors The present invention provides ethyl pyrazole compounds of formula (I): compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
US20110312910 Pharmaceutical composition based on a hepatoprotector and a prebiotic, and production and application thereof The invention relates to medicine, hepatology and pharmacology and can be used for producing and using a pharmaceutical composition based on a hepatoprotector and a prebiotic for treating and preventing liver diseases which are caused by lipid-cholesterol exchange and selected from the following group: cholelitiasis mainly with cholesterol stones, alcoholic and non-alcoholic steatohepatitis, biliary cirrhosis, cholesterol imbibition gallbladder and drug-induced and toxic liver damage. The pharmaceutical composition is administered by mouth and contains a hepatoprotector and a prebiotic taken, as an active agent, in therapeutically effective doses. The invention contributes to the liver's functional recovery in a short time and prevents disease recidivation owing to the recovery of cholesterol exchange and intestinal biocenosis as a result of the synergistic interaction of a hepatoprotector and a prebiotic, thereby also preventing hepatoprotector side effects.
US20100143381 Lysophosphatidic acid receptor targeting for lung disease The present invention contemplates that lysophosphatidic acid (LPA) may be induced by lung injury and may be responsible for aberrant wound-healing responses. For example, in a bleomycin model of pulmonary fibrosis LPAi deficient mice are protected from pulmonary fibrosis and mortality. Specifically, chemotactic-induced fibroblast responses, lung fibroblast accumulation, and vascular permeability increases were all attenuated. In contrast, however, bleomycin-induced leukocyte recruitment was preserved. These results demonstrate that LPAi activity may link pulmonary fibrosis with lung injury by mediating fibroblast recruitment and vascular leak. The present invention therefore represents LPAi as a new target to treat lung diseases including, but not limited to, fibrosis, idiopathic pulmonary fibrosis, and acute respiratory distress syndrome.
US20120093883 Method of treating and preventing neuro-olfactory triggered or aggravated illnesses or related conditions A method for treating at least one of neuro-olfactory triggered illnesses, and related conditions within a subject is provided. The method includes the steps of: a) providing a composition that includes one or more agents adapted to induce a level of anosmia/hyposmia in the subject, which level of anosmia/hyposmia is sufficient to substantially decrease olfactory sensory stimulation within the subject and a neurologic response to the stimulation that is one or both of triggering and aggravating the illness or condition; and b) applying the composition to a nasopharynx region of the subject.
US6933310 treating motor neuron diseases by administering 3-methyl-1-phenyl-2-pyrazoline-5-one or a salt thereof An object of the present invention is to provide a novel medicament with which motor neuron diseases can be treated. According to the present invention, there is provided a therapeutic agent for motor neuron diseases which comprises 3-methyl-1-phenyl-2-pirazoline-5-on or physiologically acceptable salts thereof as an active ingredient.
CN101195603A Novel crystal system of pitavastatin calcium and method for producing the same The invention relates to organic chemical and pharmacy technical field, which provides a new crystal form of (3R, 5R)-7-[2-cyclopropyl-4-(4-fluorophenyl) quinoline-3-group]-3, 5-dihydroxy-6(E)-semi-calcium heptanoate (pitavastatin calcium) for treating hypercholesterolemia or atherosclerosis, and a relative preparation method. The 2-theta value relative to the characteristic diffracted ray in X-powder diffracted pattern of the crystal form is 4.3 and 5.2, while the positions of 2-theta as 6.6, 8.6, 11.0, and 13.1 are existed with relative diffracted rays, and the water content of the crystal form is 0.5-3%.
EP1492563A2 Compositions and methods for the diagnosis and treatment of herpes simplex virus infection Compounds and methods for the diagnosis and treatment of HSV infection are provided. The compounds comprise polypeptides that contain at least one antigenic portion of an HSV polypeptide and DNA sequences encoding such polypeptides. Pharmaceutical compositions and vaccines comprising such polypeptides or DNA sequences are also provided, together with antibodies directed against such polypeptides. Diagnostic kits are also provided comprising such polypeptides and/or DNA sequences and a suitable detection reagent for the detection of HSV infection in patients and in biological samples.
WO2014004647A1 A nutritional approach to improving athletic performance and reducing injury with l-ergothioneine and/or vitamin d2 Nutritional products, compositions, functional ingredients, medical foods, pharmaceutical preparations and methods of use are disclosed for support and improvement of athletic performance (strength, flexibility, endurance, balance, and conditioning), and prevention and repair of injuries, including improving or maintaining muscle mitochondrial health, stimulating muscle mitochondrial biogenesis as well as other indications as set forth herein. In addition, pharmaceutical, nutraceutical and nutritional medical food compositions that are useful in conditions, normal or abnormal, associated with mitochondrial dysfunction and altered biogenesis in organ systems consisting of skeletal muscle, smooth muscle and cardiac muscle are also disclosed. L-Ergothioneine (also referred to as Ergothioneine or ET), Vitamin D2 (Ergocalciferol) and/or other antioxidants are disclosed for use in pharmaceutical, nutraceutical and nutritional medical food compositions for uses to stimulate production of bioactive molecules, including but not limited to glutathione, alpha synuclein, and IL-6.
WO2014001889A1 Angiotensin converting enzyme inhibitors for treating optic neuropathy or congenital optic atrophy The present invention relates to an ophthalmic composition comprising at least one angiotensin converting enzyme (ACE) inhibitor and a pharmaceutically acceptable vehicle for use as an ophthalmic neuroprotector in treating an optic neuropathy or congenital optic atrophy.
US7270818 Treating brain disorder by administering a therapeutically effective amount of antisense oligonucleotide; preventing the formation of Alzheimer senile plaques Methods of treating and/or prophylaxis Alzheimer's disease by preventing the formation of cerebral amyloid due to the growth and disruption of dense microspheres (DMS) are disclosed utilizing medicaments that are effective in preventing or inhibiting the growth and disruption of DMS.
WO2009137493A1 2-substituted benzofuran compounds to treat infection with hepatitis c virus Compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, including all crystalline forms and pharmaceutically acceptable salts thereof, which are useful in pharmaceutical formulations for the treatment or prevention of hepatitis C virus infections and diseases associated with such infections.
EP1528921A2 Methods for treatment and prevention of gastrointestinal conditions Therapeutic methods for the prevention ad treatment of conditions and diseases of the gastrointestinal tract involving an overproduction of nitric oxide by inducible nitric oxide synthase are described, the methods including administering to a subject in need thereof a therapeutically effective amount of a selective inhibitor of inducible nitric oxide synthase (iNOS). The methods also include the use of selective inhibitors of iNOs in combination with other therapeutic agents, including antimicrobial agents and antisecretory agents.
WO2014096497A1 Liquid carbocisteine formulations having improved properties The invention relates to liquid carbocisteine formulations having improved organoleptic properties and stability.
WO2008094574A3 Furanone compounds and methods of making and using the same The invention features compounds of the general Formula (I). Compounds of Formula (I) possess unexpectedly high affinity for Alk5 and/or Alk4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders.
EP1852436A1 Process for production of carbapenem derivative and crystalline intermediate therefor An object of the present invention is to provide a carbapenem synthetic intermediate which is advantageous in an industrial process. There are provided a process for producing Compound (I), or a pharmaceutically acceptable salt, or a solvate, or a crystal thereof, comprising reacting Compound (III) and Compound (IV) in the presence of the secondary amine, and a benzyl alcoholated crystal of Compound (I). There are further provided a method of deprotecting Compound (I) with a Pd catalyst, and a crystal of Compound (IV).
US7754236 polyester-based film substrate have specified surface roughness on the side that a drug-containing adhesive layer is laminated thereon; free from any migration of a drug into a substrate; bonding strength, no adhesive residue when peeled off skin; for narcotic analgesic fentanyl The present invention relates to a patch which is free from any migration of a drug into a substrate and has favorable anchoring properties between the substrate and adhesive layer, in which the drug containing adhesive layer firmly adheres onto the substrate and which gives no adhesion residue when applied to the skin and then peeled off. Namely, a patch comprising a substrate made of a polyester-based film and a drug-containing adhesive layer laminated thereon wherein the surface roughness (also known as “the central line mean roughness” or “Ra”) of the polyester-based film surface in the side in contact with the adhesive layer is from 0.05 to 0.8 μm is provided.
US20080064724 Composition Comprising Methylphenidate and Another Drug A process of treating a subject that is undergoing methylphenidate therapy and concomitant therapy with another drug undergoes or interferes with P450 metabolism wherein the methylphenidate is d-threo-methylphenidate.
US6841550 Benzoxazine and benzothiazine derivatives and their use in medicines The invention relates to compounds of formula (I) and their tautomeric and isomeric forms and salts, as well as to a method for producing said compounds and their use in medicines.
CN102861086A Application of Houttuynoid E in medicine for treating ovarian cancer The invention discloses application of Houttuynoid E in preparation of a medicine for treating human ovarian cancer, belonging to the technical field of new application of medicine. The invention discovers that Houttuynoid E has the remarkable inhibitory effects on the growth of human ovarian cancer cell strains, including HO-8910, HOC1 and OVAC through the evaluation of in vitro MTT antineoplastic activity. Therefore, Houttuynoid E can be used for preparing the anti-ovarian cancer medicine and has good development and application prospects. The application of Houttuynoid E in preparation of the medicine for treating human ovarian cancer provided by the invention is disclosed firstly. The skeleton type belongs to new skeleton type, and the inhibitory activity of Houttuynoid E on human ovarian cancer cells is unexpectedly strong.
CN102731296A Rosmarinic acid derivative, its preparation method, and its application in preparation of antitubercular medicines The invention provides a rosmarinic acid derivative which comprises compounds 1-47 and their R-isomers or S-isomers. The structural general formula of the derivative is represented by a formula in the specification; and in the formula, R1, R2, R3 and R4 are defined in the specification. According to in-vitro anti-Mycobacterium tuberculosis experiments of the rosmarinic acid derivative of the invention, a medicine to be detected and a positive contrast medicine are respectively added to a small bottle containing a liquid medium in a continuous two-time dilution manner, a certain bacterium amount of Mycobacterium tuberculosis standard strains H37Rv is inoculated and is cultured for 14 days at 37DEG C, and the minimum inhibitory concentration (MIC) of each medicine to the Mycobacterium tuberculosis is observed. And experiment results show that the compounds in the invention have good anti-Mycobacterium tuberculosis activities, so the compounds can be used for preparing medicines for treating tuberculosis infection, and have large clinical application values. The invention provides a preparation method of the rosmarinic acid derivative.
CA2602787A1 Pyridine-3-carboxamide derivatives as cb1 inverse agonists The present invention relates to compounds of the formula (I) wherein X and R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.
CN102988409A Application of dextran sulfate in preparation of medicine for treating serious hepatitis The invention discloses novel application of dextran sulfate in preparation of a medicine for treating serious hepatitis. The medicine can be used for inhibiting the inflammatory response in the pathogenesis of serious hepatitis in order to inhibit the pathogenesis of serious hepatitis or exacerbating of symptoms. The dextran sulfate shows a greater treatment effect by virtue of an animal model under the induction of endotoxin and D-galactosamine; and simultaneously, the medicines adopted are easy to obtain, low in price, stable in quality, convenient in storage and conveying, and wide in application prospect.
CN101601676A Compound oxycycline soluble powder for treating fowl spirochetosis infection and preparation method thereof The invention discloses compound oxycycline soluble powder for treating fowl spirochetosis infection and a preparation method thereof, and aims to provide the compound oxycycline soluble powder for treating fowl spirochetosis infection with quick response, safe use, efficiency and high activity, and the preparation method thereof. The soluble powder comprises the following compositions in percentage by weight: 5 to 15 percent of oxycycline, 5 to 15 percent of maquindox, 5 to 20 percent of paracetamol, 2 percent of vitamin K3, and the balance of anhydrous dextrose. The soluble powder adopts the oxycycline and the maquindox to reduce medicinal resistance of pathogenicbacteria, improves the treatment effect, has quick response and prominent curative effect of treating the fowl spirochetosis infection by combining with the antipyretic paracetamol and the vitamin K3 with hemostatic function, and can effectively prevent infection of other bacteria.
WO2007140551A2 Treatment of cnidaria intoxication with vanilloid receptor antagonists The present invention relates to the use of vanilloid receptor (VR) antagonists, and more particularly vanilloid receptor 1 (VR1) antagonist, as analgesics in the treatment and/or prohylaxis of cnidaria envenomations.
CN101732440A Raspberry extract and raspberry element obtain by separation thereof and application thereof The invention relates to medical technical field, relating to raspberry extract extracted from Rubus chingii Hu and raspberry element obtained from separating the raspberry extract and the application of the two in preparing medicines for treating and preventing chronic nephritis, kidney-yang deficiency and osteoporosis. The raspberry element has the following chemical structural formula. The raspberry extract and the raspberry element have activity of treating and preventing chronic nephritis, kidney-yang deficiency and osteoporosis, thereby being capable of preparing medicines for treating and preventing chronic nephritis, kidney-yang deficiency or osteoporosis.
CA2627910A1 Substituted cycloalkylpyrrolones as allosteric modulators of glucokinase The present invention relates to compounds of Formula (I), (I) methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating glucokinase mediated disorders. More particularly, the compounds of the present invention are glucokinase modulators useful for treating disorders including, but not limited to, type II diabetes.
CN103356645A Application of Chukrasone A in preparation of medicines for preventing or treating renal insufficiency The invention relates to an application of Chukrasone A in preparation of medicines for preventing or treating renal insufficiency and belongs to the technical field of new applications of medicines. The application of the Chukrasone A in preparation of medicines for preventing or treating renal insufficiency provided by the invention is disclosed for the first time. As the framework type is a brand new framework type and the inhibitory activity of the Chukrasone A to renal insufficiency is unimaginably strong, the probability of giving any enlightenment by other compounds does not exist. The Chukrasone A has remarkable substantial characteristics and meanwhile has remarkable progress in prevention and control of renal insufficiency.
CN103142525A Olanzapine gastric soluble tablets and preparation method thereof The invention relates to olanzapine gastric soluble tablets and a preparation method thereof. Particularly, the olanzapine gastric soluble tablets comprise the following components in percentage by weight: 2 to 15 percent of olanzapine, 40 to 82 percent of mannitol, 5 to 30 percent of microcrystalline cellulose, 0.5 to 2 percent of silicon dioxide, and 0.5 to 3 percent of magnesium stearate. The olanzapine gastric soluble tablets have the overall effects of quick dissolubility and stable preparation quality, and do not have the remarkable moisture absorption phenomenon when being placed in the air for a long time. The preparation method is simple in process steps, low in cost and energy consumption and short in production cycle, and thus is suitable for wide popularization and application.
US20110077249 1,2,4-triazolylaminoaryl (heteroaryl) sulfonamide derivatives 1,2,4-Triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I), pharmaceutically acceptable salts thereof, processes for the manufacture of 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives and pharmaceutical compositions containing 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives are disclosed: The 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I) possess cell cycle inhibitory activity and are accordingly useful for their anti cell proliferation (such as anti cancer) activity.
CN102824327A Medicinal composition of agomelatine-containing enteric-coated tablets The invention relates to a medicinal composition of agomelatine-containing enteric-coated tablets. The medicinal composition is mainly composed of a medicine-containing tablet portion and an enteric coating portion, wherein the content of an active component-agomelatine is 1 mg-50 mg. The enteric-coated tablets provided by the invention can be used for treating depression and anxiety, have the functions of adjusting sleeping rhythms and biological clocks, and have the advantages of low content of the main medicine and high bioavailability.
WO2008020255A1 Benzo[1,2,3]thiadiazine derivatives (I) The present invention relates to new benzo[1,2,3]thiadiazine-1,1 dioxide derivatives of the general Formula (I), medicament containing such compounds and the use thereof in the medicin Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the gener Formula (I) are suitable for the prevention or treatment of the disease of the central nervous system.
CN1853629A Berberine dripping balls and preparation thereof A dripping pill of berberine is prepared from the berberine through proportionally mixing it with matrix (polyoxyvinyl monostearate), heating until the mixture is fused, stirring, dripping in condensing liquid and coating.
WO2005082847A1 Bicyclo derivative Disclosed is a novel bicyclo derivative having excellent DPP-IV inhibitory activity which is represented by the general formula (1) below or a pharmacologically acceptable salt thereof. (Specific examples thereof include (2S,4S)-1-[[N-(4-methylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile.)
US20110065777 DOUBLE-STRANDED RNA (dsRNA) AND METHOD OF USE FOR INHIBITING EXPRESSION OF A FUSION GENE Specific inhibition of expression of a fusion gene in mammals occurs using a short, double-stranded ribonucleic acid molecule (dsRNA). The dsRNA comprises two separate non-linked RNA strands, an 51 strand and a complementary strand. The strands are 20 to 23 nucleotides in length, and the 51 strand is complementary to the fusion junction of the AML-1/MTG-8 fusion gene. The dsRNA also comprises at least 3 nucleotides on each side of the fusion junction. The dsRNA can be introduced into and maintained in a mammalian cell under conditions and for a time sufficient to obtain degradation of mRNA of the fusion gene to inhibit expression of the fusion gene. The dsRNAs and methods described are useful for treating diseases caused by chromosomal aberrations, particularly malignant diseases such as lymphoma and leukemia.
US20110224240 Methods of treating cancer and related diseases Disclosed are orally bioavailable compounds effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, such as in cancer and related diseases.
WO2008077557A1 8-ethinylxanthine derivatives as selective a2a receptor antagonists Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof (Ia) and their use as medicines, for example in the treatment of dopamine-related movement disorders.
EP2784061A1 Acyl-hydrazone and oxadiazole compounds, pharmaceutical compositions containing the same and uses thereof The present invention relates to acyl-hydrazone compounds, in particular 3,4,5-trimethoxyphenyl-hydrazide derivatives, as well as the oxadiazole analogs thereof and other similar compounds, and to the pharmaceutical use of the same for the treatment of various diseases associated with cell proliferation, such as leukemias, including acute lymphoblastic leukemia (ALL), tumours and inflammation. Acyl-hydrazones have been obtained having activity similar to that of the compound used as a standard in experiments (colchicine). The greater selectivity of the compounds according to the invention is an important feature, associated with fewer side effects than the pharmaceuticals used at present in clinical treatments. The synthetised acyl-hydrazones, more particularly the compounds 02 and 07, exhibited important anti-leukemic activity, which suggests 02 and 07 as candidates to pharmaceutical prototypes, or to pharmaceuticals for the treatment of leukemias, in particular acute lymphoblastic leukemia (ALL), tumours and other proliferative diseases, such as inflammation. The action mechanism of the most active compounds was determined by using DNA microarrays and subsequent tests indicated by the chip, besides selectivity studies in healthy human lymphocytes.
US20090010919 Diagnostics and Therapeutics for Diseases Associated With Fibroblast Activation Protein (Fap) The invention provides a human FAP which is associated with the cardiovascular diseases, respiratory diseases, cancer, dermatological diseases, metabolic diseases, inflammation, gastroenterological diseases, hematological diseases, muscle skeleton diseases, neurological diseases, urological diseases and endocrinological diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular diseases, respiratory diseases, cancer, dermatological diseases, metabolic diseases, inflammation, gastroenterological diseases, hematological diseases, muscle skeleton diseases, neurological diseases, urological diseases and endocrinological diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of FAP as well as pharmaceutical compositions comprising such compounds.
CN101234112A New purpose of cation carbazoles compounds The invention discloses a new purpose of cationic carbazole compound, which is the application of cationic carbazole compounds or the salts thereof acceptable in pharmacy in preparing preventive and/or therapy tumor drugs. The cationic carbazole compound is compound (I) or (II). The test of anticancer activity in vitro shows that the cationic carbazole compound has better inhibitory effects on both human hepatoma cells and human colon cancer cells.
US20120157494 Isoindolyl compounds Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
US20080096937 For example, 2-{4-[(2-chloro-benzyl)-ethyl-amino]-phenyl}-1,1,1,3,3,3-hexafluoro-propan-2-ol; the compounds bind to and selectively activate LXR alpha and LXR beta; used to treat diseases such as atherosclerosis and diabetes The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.
US20120270916 Topical formulations for treating neuropathy Compositions for the topical or transdermal treatment of neuropathy. More particularly, transdermal or topical compositions including a combination of ingredients that provide a surprising degree of effective relief from the symptoms of peripheral neuropathy are described.
CN101434580A Mesaconitine acylated product nitrous oxide, preparation and use The invention discloses a preparation method of a nitrogen oxide (with a compound structure shown as the picture) of an aconitine acylate product and an application thereof, pertaining to the technical field of medical and pesticide synthesis. The preparation method of the nitrogen oxide of the aconitine acylate product comprises the steps that the aconitine acylate product which is served as a raw material and a metachloroperbenzoic acid (mCPBA) which is served as an oxidant are stirred for reaction for 3 hours to 20 hours at temperature of 10 DEG C to 40 DEG C; extraction is carried out after pH value is adjusted to between 8 to 10; then the nitrogen oxide of the aconitine acylate product is obtained by means of column chromatography and separation after pressure reduction and distillation. The compound has obvious desinsection activity and remarkable activities of easing pain, resisting against arrhythmia and tumors, and the like, and can be used for developing new products in respect of medicines, pesticides, etc. In the formula, R refers to alkyl with 1 to 4 carbon atoms while R1, R2 and R3 refer to hydrogen atoms, hydroxyl, aliphatic acyl or aromaticacyl radical.
CN103099787A Vitamin C dry suspension The invention relates to a dry suspension, in particular to a vitamin C dry suspension.
CN102920678A Olanzapine solid preparation and preparation method thereof The invention relates to an olanzapine solid preparation and a preparation method thereof. The preparation comprises (a) a table core treated through micronization, (b) a drug layer coated surround the outer layer of the tablet core, wherein an average particle size of the drug layer containing the olanzapine is 0.1-45 mum, and (c) a coating layer coated surround the olanzapine coating layer. Optionally the preparation further comprises other pharmaceutically acceptable excipients. The preparation has characteristics of rapid disintegration and absorption in oral cavity, easy taking, improved patient medication compliance and high bioavailability so as to achieve the purpose of disease control rate improvement.
WO2009016632A1 Edible fat composition for enhancing bone strength Disclosed is describes a method of increasing bone strength and/or increasing bone resistance to bending and/or improving bone architecture and/or maintaining bone status in a human, comprising administering to said human a composition comprising a fat source, wherein said fat source is a triglyceride fat source comprising triglycerides with 15-55% palmitic acid moieties out of the total fatty acids, and wherein the level of palmitic acid moieties at the sn-2 position of the glycerol backbone is at least 30% (w/w) of total palmitic acid. Said method is particularly intended for subjects at risk of impaired bone strength. Further disclosed is said fat source, as well as food articles and a commercial package comprising the same.
EP2384623A1 Powder composition for the prevention and treatment of animal hoof diseases A powder composition for the prevention and treatment of animal foot diseases is described, as well as the uses thereof. In particular, the present invention relates to a composition for preventing animal hoof infections and for treating inflammatory states of the hoof.
US20130035332 Substituted 1,3-Benzothiazol-2(3H)-Ones and [1,3]Thiazolo[5,4-B]Pyridin-2(IH)-Ones as Positive Allosteric Modulators of MGLUR2 The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
CN103408537A 5-substituted dihydrobenzofuran-imidazolium salt compound and preparation method thereof The invention discloses a 5-substituted dihydrobenzofuran-imidazolium salt compound and a preparation method thereof. The preparation method comprises the following steps of: performing Vilsmeier reaction by taking 2,3-dihydrobenzofuran as a raw material, thereby synthesizing 5-carboxaldehyde dihydrobenzofuran, reducing the 5-carboxaldehyde dihydrobenzofuran into 5-benzyl alcohol substituted dihydrobenzofuran in an alcohol by using sodiumborohydride, and then converting the 5-benzyl alcohol substituted dihydrobenzofuran into methanesulfonate, next, carrying out a reflux reaction between the methanesulfonate and imidazolium or benzimidazole in a solvent, thereby synthesizing 1-(substituted dihydrobenzofuran) imidazolium, and finally, on the basis, reacting the 1-(substituted dihydrobenzofuran) imidazolium with a halide to synthesize the 5-substituted dihydrobenzofuran-imidazolium salt compound. According to the invention, a pharmacophore with remarkable anti-tumor activity in a natural product is used as a precursor and then design and synthesis of anti-tumor medicine molecules are carried out, and consequently, the synthesized compound has excellent in-vitro anti-tumorous cytotoxin activity. Researches show that the compound has excellent in-vitro anti-cancer biological activity when the imidazolium structure unit is 5,6-dimethyl benzimidazole and the substituent group thereof on the site of 3 is 2-bromobenzyl, naphthoyl methyl or 4-bromophenacyl.
US20080207750 Use of N-Chlorotaurine for Treatment of Oozing Tissue Deficiencies A pharmaceutical composition containing N-chlorotaurine is administered to a mammal to treat oozing tissue deficiencies.
WO2009061852A2 Modulation of factor 9 expression Disclosed herein are antisense compounds and methods for decreasing Factor 9 and increasing clotting time in an individual in need thereof. Examples of disease conditions that can be ameliorated with the administration of antisense compounds targeted to Factor 9 include thrombosis, embolism, thromoboembolism such as deep vein thrombosis, pulmonary embolism, myocardial infarction, and stroke.
CA2292775C Cyanoguanidines as cell proliferation inhibitors The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C5-C14 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carboxy, C1-C4 alkoxycarbonyl, di(C1-C4 alkoxy)-phosphinoyloxy, amino, C1-C4 alkoxycarbonylamino or tetrahydropyranyloxy; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.
CN103301090A Preparation method of genistein targeted nanometer particle The invention discloses a preparation method of a genistein targeted nanometer particle, which belongs to the technical field of pharmacy. The preparation method comprises the following steps of: mixing trisodium citrate dehydrate, sodium hydroxide, ferrous sulfate heptahydrate, sodium tripolyphosphate and deionized water; adding a polyethylene glycol 400 solution of genistein; adding chitosan under stirring; centrifuging and separating after 2 hours to obtain the yellowish-brown genistein targeted nanometer particle. The product prepared by the preparation method disclosed by the invention can be used for changing the distribution of the drug in the human body and the dynamic characteristic of the drug, so that the drug is prevented from distributing broadly in the body and diffusing quickly; the targeted orientation of the drug can be used for reducing the drug exposure of the normal tissue, so that the side and toxic effect is lowered, and the treatment effect of the drug is improved.
US20120108823 Anti-francisella agents A series of celecoxib derivatives defined by Formula I: were prepared and evaluated for their ability to inhibit the gram-negative bacteria Francisella tularensis. Pharmaceutical compositions including celecoxib derivatives and their use in methods for treating or preventing infection by Francisella tularensis in a subject are described.
EP1250130A4 Propofol formulation with enhanced microbial inhibition A sterile, stable pharmaceutical formulations of oil-in-water emulsions of Propofol containing no preservative are provided that comprise optimal amounts of egg lecithin and soybean oil, with a suitable pH range to prevent significant growth of microorganisms for at least 24 hours after adventitious, extrinsic contamination. The lower pH in the formulation has shown the most antimicrobial activity. The reduced amount of fat in the formulation also allows chronic sedation over extended periods of time with a reduced chance of fat overload in the blood.
US20100215730 Compositions for Nasal Administration of Phenothiazines Provided herein are pharmaceutical compositions comprising phenothiazines or derivatives thereof that are formulated for nasal administration. Also provided herein are methods of utilizing the same.
EP1927353A1 Remedy for corneal diseases A therapeutic agent for a corneal disease comprising ozagrel or a salt thereof as an active ingredient is provided. The purpose is to find a substance capable of effectively treating/ameliorating a corneal disease which has been increased in the number of cases thereof in recent years and to provide a therapeutic agent for a corneal disease comprising the substance as an active ingredient.
WO2006013457A3 Gad2 gene for possible treatment of nervous system disorders The present invention regards methods and formulations for treatment of neurological and behavioural disorders eating disorders. More particularly, the present invention is applied to increase appetite in anorexic individuals or individuals with other eating disorders where an increase in appetite may be therapeutic. In the present invention, the GAD2 gene is inserted with a strong promoter, such as in an adenoassociated virus, and this is in turn administered into the paraventricular nucleus and other areas of the hypothalamus of anorexic individuals.
EP1313703B1 Prodrugs to nmda receptor ligands The invention relates to compounds of the general formula (I) wherein R is a) -C(O)(CH2)nC(O)OH, b) wherein R1 is -N(R?2)(R3) and R2/R3¿ are independently from each other hydrogen or lower alkyl, or is a cyclic tertiary amine, optionally substituted by lower alkyl, c) -P(O)(OH)¿2?, or is d) -C(O)(CH)2)nNHC(O)(CH2)nN(R?2)(R3¿); and n is 1, 2, 3 or 4; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used as prodrugs for the parentcompound of formula (II) which are useful in the treatment of NMDA receptor-related diseases.
US20110117108 Treatment and prevention of cancerous and pre-cancerous conditions of the liver, lung and esophagus The invention relates to the treatment and/or prevention of cancerous and/or, precancerous conditions of the liver, lung and esophagus by actively and/or passively immunizing a patient against the peptide hormone gastrin and/or a gastrin receptor, e.g., the CCK-B/gastrin receptor. The immunizations of the invention may be employed as a monotherapy, an adjunctive therapy, or as part of a combination therapy.
WO2009135495A1 Method for treating cognitive deficits The invention relates to methods of treating cognitive dysfunction and improving cognitive functioning comprising the administration of tran5-4-((1R,3S)-6-chloro-3-phenylindan-1-yl)- 1,2,2-trimethylpiperazine or a pharmaceutically acceptable salt thereof to a patient in need thereof. Moreover the invention relates to an improved binder in a composition comprising 4- ((1R, 3S)-6-chloro-3-phenylindan- 1 -yl)- 1,2,2-trimethylpiperazine.
US20120058114 ERBB2 antibodies comprising modular recognition domains Antibodies containing one or more modular recognition domains (MRDs) that can be used to target the antibodies to specific sites are described. The use of antibodies containing one or more modular recognition domains to treat disease, and methods of making antibodies containing one or more modular recognition domains are also described.
WO2007141571A3 Aminothiazole derivatives as inhibitors of mark Compounds of formula (I): inhibit microtubule affinity regulating kinase (MARK) and therefore find use in treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.
US20080287418 Extended Release Compositions and Methods for Their Manufacture Extended release formulations of quetiapine and its pharmaceutically salts, and methods for manufacture of the formulations, may include the use of polymers selected for their physical and chemical characteristics. The formulations may include polymers selected to cause solid dosage forms of the formulations to conform to preselected quetiapine release criteria. The formulations may include non-polymer materials that may affect quetiapine release.
CN102836150A Drug combination containing borneol The invention belongs to the technical field of medicines, and provides a drug combination containing borneol. The drug combination comprises germacrone, furanodiene, curdione, Beta-elemene, curcumenol, curzerene and borneol. The drug combination contains definite components which is controllable in quality; the drug combination can control the content of camphol in borneol so as to improve the plasma concentration and the mucous membrane absorption rate of the drug combination; the drug combination can be used for preparing suppository, ointments, capsules, effervescent tablets, gelata, lotion, film agents or foaming agents; and the drug combination can achieve an excellent therapeutic effect on diseases such as HR-HPV (High Risk-Human PapillomaVirus) and/or LR-HPV (Low Risk-Human PapillomaVirus) and cervical diseases, and is suitable for clinical wide application.
EP2128154A1 Benzimidazole compound and pharmaceutical use thereof Provided is an ORL-1 receptor agonist having improved bioavailability based on superior metabolic stability and strong and high selectivity, as compared to conventional compounds. A compound represented by the formula (I) wherein each symbol is as defined in the Claims.
US20130079380 Method and Composition for Administering Bioactive Compounds Derived From Morinda Citrifolia This invention relates to a method and composition for providing in various health benefits by administering various bioactive compounds derived from the plant Morinda cirtrifolia to individuals. This invention relates to using one or more of the following: Noni Leaf Extract; Noni Leaf Juice; and/or Roast Leaf More particularly this invention relates to administering one or more of the following: Pyro-phorbide a, Pheophorbide a, Purpin 7, and/or Pheophorbide all which may be derived from Noni leaf extract, Noni leaf juice, and/or Roast leaf Moreover, the foregoing formulations result in alleviating pain and inflammation.
CN103690489A Breviscapine composition nano-particle and preparation method thereof The invention belongs to the field of pharmacy, and relates to a breviscapine composition nano-particle and a preparation method thereof. The provided novel breviscapine composition nano-particle is prepared by a solution containing the breviscapine, a polymer, a surfactant and a solvent with the adoption of an electrostatic spraying technology. The composition preparation device is simple, the parameters are controllable, the drug loading capacity is high, , the direct and continuous nano-particles with uniform particle size distribution can be obtained, the specific surface area is increased, and the dissolution in vitro and bioavailability of the breviscapine are improved remarkably.
CN101108845A Novel method of producing strontium ranelate heptahydrate The invention relates to a new preparation method of strontium ranelate heptahydrate. The products produced by the method have water content of 19.0 per cent to 20.4 per cent and the relevant substances are lower than 0.5 per cent. The strontium ranelate heptahydrate produced by the method is stable under room temperature, has little water content differences between batches and is kept for a long time under natural environment with unchangeable moisture, content and relevant substances. The method is characterized in that: (1) the reflux of the 2-[N, N- 2(carboxymethyl)amino]-3-cyano-group-4-thiopheneacetic-5-carboxylic acid tetra ester (b) is carried out in the proper sodium hydroxide aqueous solution of alcohol for 5h to 6h and the pH value is kept over 10 during hydrolysis; (2) the ethanol of 20 per cent to 60 per cent is added and then the strontium chloride aqueous solution with 2times to 2.5times molal weight is directly added, precipitates the crystal, is filtered and dried; (3) water is added to carry out the reflux and the little salt packed in the crude product is removed, and the product is collected through heat filtration. The invention discloses the drug combination containing the strontium ranelate heptahydrate which is used for the treatment of osteoporosis of women after menopause.
WO2011152657A2 Acetyl-l-carnitine malate, process for preparing the same, and pharmaceutical composition comprising the same The present invention relates to acetyl-L-carnitine malate, a process for preparing the same, and a pharmaceutical composition comprising the same. The acetyl-L-carnitine malate of the present invention has good stability, solubility, and non-hygroscopicity to be effectively used for preparing a pharmaceutical composition.
WO2008071974A2 Use of pi3k m-tor and akt inhibitors to induce f0xp3 expression and generate regulatory t cells The invention relates to a method of inducing Foxp3 expression in a T cell comprising (i) stimulating a T cell (ii) inhibiting signalling via PBK alpha or PBK delta or m-TOR or Akt in said T cell, wherein said inhibition is commenced 10 to 22 hours after the stimulation of (i). The invention also relates to certain uses of PBK inhibitors, PBK inhibitors for particular uses, and kits.
CN101732235B Method for preparing solid dispersion of tamoxifen citrate The invention discloses a method for preparing an oral solid preparation of tamoxifen citrate, including: firstly preparing the solid dispersion of the tamoxifen citrate by the tamoxifen citrate, polyethylene glycol-6000 and a flow aid, then mixing uniformly the prepared solid dispersion of the tamoxifen citrate and a filler or a disintegrating agent or skeletal material according to a ratio and tabletting, preparing common tablets or dispersible tablets or sustained-release tablets; or directly filling the prepared solid dispersion into capsules or mixing uniformly with calcium hydrogen phosphate according to a ratio then filling into capsules. The invention can conveniently prepare the oral solid preparation such as common tablets, dispersible tablets, sustained-release tablets and capsules having high bioavailability and good absorbability, and the dissolution of the tamoxifen citrate can stably reach over 95 percent; and the preparation method has the advantages of low cost, easy operation, no special requirement on equipment, suitability for mass production and the like, and establishes a good relationship between the disintegration, dispersion and release speed and the medical dissolution of the solid dispersion of tamoxifen citrate.
CN103599081A Novel niacin compound slow-release preparation for treating hyperlipoidemia The invention provides a novel niacin compound slow-release preparation for treating hyperlipoidemia. The novel niacin compound slow-release preparation comprises a quick-release part and a slow-release part, wherein the quick-release part comprises statins and pharmaceutical excipients; the slow-release part comprises niacin, polyvinylpyrrolidone k90 and pharmaceutical excipients; the weight ratio of the statins to niacin in the preparation is 1:(10-100), the weight ratio of polyvinylpyrrolidone k90 to niacin in the slow-release part is 1:(20-80), and the dosage form of the compound preparation is slow-release coating tablets. The compound preparation provided by the invention is suitable for treating hyperlipoidemia of Asian people. Compared with the existing niacin statin slow-release preparation, the compound preparation provided by the invention is less in the content of statins and can achieve a very good treatment effect at the same time, so that the toxic and side effects of medicaments are greatly reduced.
CN102010418A High-camptothecin compounds and use thereof as medicaments The invention relates to the technical field of medicaments, in particular to novel high-camptothecin compounds and use thereof as anti-tumor medicaments. The compounds have the structure shown in a general formula (I) and comprise optical isomers, racemes, trans-isomers and any mixture or pharmaceutical salts thereof in the forms. The compounds have the function of inhibiting the activity of topoisomerase and can be used for preparing the anti-tumor medicaments.
CN101134046A Application of TLR4 and TLR9 agonist compound in the restraint of tumour metastasis The present invention discloses the application of compound of TLR4 excitant as LPS from Porphyromonas gingivalis and TLR9 excitant of E.coli 0111:B4 LPS in preparing medicine for preventing tumor metastasis, and is especially the application of TLR4 excitant and TLR9 excitant in inhabiting pulmonary tumor metastasis. The present invention discloses one kind of medicine composition including TLR4 excitant, TLR9 excitant and pharmaceutically acceptable carrier. The experiment with high pulmonary tumor metastasis mouse model shows that the compound of TLR4 excitant and TLR9 excitant can inhibit the metastasis of mouse pulmonary tumor caused by melanoma.
US6984661 for preventing, Syndrome X, diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, atherosclerosis, and other disorders related to Syndrome X and cardiovascular diseases; peroxisome proliferator activated receptor (PPAR) The present invention is directed to compounds of the structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof: Formula I (a) R1, R2 and R6 are each independently selected from the group consisting of hydrogen, C1-C8 alkyl substituted C1-C8 alkyl, aryl-C0-4-alkyl, substituted aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, substituted heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and substituted C3-C6 cycloalkylaryl-C0-2-alkyl; (b) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S; (c) Y is C, O, S, NH or a single bond; and (d) E is selected from the group consisting of hydrogen, C(R3)(R4)A, A, (CH2)n COOR19 and substituted (CH2)n COOR19.
EP1387843B1 Method for obtaining pioglitazone as an antidiabetic agent A method for obtaining antidiabetic of formula (I), wherein the method comprises condensing of a 4-derivatized phenol or phenolate of general formula (II), wherein R is an amino group-containing organic residue, selected from the group comprising a residue of the following formula -NHR3, wherein R3 is hydrogen or a protecting group, which is removed before further treatment, and a residue of general formula (A), wherein Rb represents a carboxy group either in the free acid form or in the form of a salt or ester or another functional derivative or the nitrile group CN, and M represents a hydrogen or alkali metal atom, with a pyridine base of general formula (III), wherein Z is a leaving group other than a halogen, wherein, before or after carrying out the condensation, the following operations are carried out: (a) diazotizing the amino group present in organic residue R; (b) converting the diazotised residue R into a derivative of 2-halopropionate or 2-halopropionitrile of formula (B), wherein Rb is as defined above and X is a halogen; (c) cyclizing the derivative of 2-halopropionate or 2-halopropionitrile with thiourea; (d) hydrolysing the resulting imine thus giving pioglitazone of formula (I).
WO2012093855A3 Novel flavi mycin compound, antifungal composition including same, and method for producing same The present invention provides a flavi mycin compound represented by Formula 1 or Formula 2, an isomer thereof, a derivative thereof having peptide deformylase-inhibitory activity, a pharmaceutically acceptable salt thereof, or an antifungal composition including as an active ingredient a strain, a bacteria, or a culture thereof, which produce the flavi mycin compound that is represented by Formula 1 of Formula 2, and provides a composition for suppressing peptide deformylase activity. The present invention also provides a method for preventing or treating a microorganism-contracted disease using the antifungal composition, a method for sterilizing a microorganism or rendering same bacteriostatic, and a method for producing the compound or the derivative thereof using an Aspergillus flavips F543 strain. The compound or the strain of the present invention strongly inhibits the activity of the peptide deformylase, thereby having a strong antifungal property against a pathogenic microorganism or antibiotics-tolerant bacteria, and in particular, can be useful in treating contagious diseases which are caused by super bacteria by exhibiting antifungal activity to metacillin-resistant Staphyloscoccus aureus and quinolone-resistant Staphyloscoccus aureaus.
CN101570521B Preparation method and medical application of 4-tert-butyl-6-phenyl-2-amino-6H-1,3-thiazine salt The invention discloses a preparation method and medical application of 4-tert-butyl-6-phenyl-2-amino-6H-1,3-thiazine salt. The preparation method of the 4-tert-butyl-6-phenyl-2-amino-6H-1,3-thiazine salt comprises the steps of: stirring 0.010 mol of 1-phenyl-4,4-dimethyl pentene-3-ketone, 0.012 mol of thiourea and 0.011 mol of acid in an organic solvent at a temperature of between 30 and 80 DEG C, performing TLC detection on reaction process, completing reaction, filtering, washing and drying the obtained product and obtaining the 4-tert-butyl-6-phenyl-2-amino-6H-1,3-thiazine salt (I). The 4-tert-butyl-6-phenyl-2-amino-6H-1,3-thiazine salt (I) can be medically used for preparing influenza virus neuraminidase inhibitors. In a formula, HX is hydrochloric acid, phosphoric acid, hydrobromic acid, sulphuric acid, trifluoroacetic acid or methanesulfonic acid, and Y is Cl, Br, CH3, Et, CF3, OCH3 or OEt.
US7279493 cyanoiminopiperazines which inhibit vanilloid receptor 1 function in a cell A compound of formula: wherein A, Ar, R3, R6, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Cyanoiminopiperazine Compound”), compositions comprising an effective amount of a Cyanoiminopiperazine Compound, and methods for treating or preventing pain, urinary incontinence, an ulcer, inflammatory-bowel disease, irritable-bowel syndrome, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cyanoiminopiperazine Compound are disclosed.
US20080279920 Compositions For Treating Respiratory Viral Infections and Their Use The invention provides siRNA compositions that interfere with viral replication in respiratory viral infections, including respiratory syncytial virus and avian influenza A, including the H5N1 strain. The invention further provides uses of the siRNA compositions to inhibit expression of viral genes in respiratory virus-infected cells, and to uses in the treatment of respiratory virus infections in a subject. Generally the invention provides polynucleotide that includes a first nucleotide sequence of 15 to 30 bases that targets the genome of a respiratory syncytial virus or an influenza A virus, a complement thereof, a double stranded polynucleotide or a hairpin polynucleotide. Additionally the invention provides vectors, cells and pharmaceutical compositions containing siRNA sequences.
US20120225909 Indazole analog [Objective] To provide a drug that selectively stimulates the β3-adrenergic receptors, particularly a drug capable of preferentially stimulating the β3-adrenergic receptors over the α1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like. [Solution] Indazole analogs represented by the general formula (I) or a salt thereof. Drugs that contains these indazole analogs or a salt thereof as the active ingredient.
US20090170953 Indentification of compounds that inhibit replication of human immunodeficiency virus The present invention relates to the discovery of a novel class of compounds that inhibit the replication of human immunodeficiency virus (HIV) and approaches to identify these compounds. More specifically, it has been found that enzymatically prepared alpha-hydroxyglycinamide and synthetically prepared alpha-hydroxyglycinamide inhibit the replication of HIV in human serum. Embodiments include methods to identify modified glycinamide compounds that inhibit HIV, methods to isolate and synthesize modified glycinamide compounds, and therapeutic compositions comprising these compounds.
WO2012165547A1 Method for manufacturing pyrazole derivative The present invention provides a prolinamide compound useful as a drug or the like and an industrially advantageous method for producing a piperazinyl pyrazole compound that is a production intermediate of the prolinamide compound. Specifically, the invention is a method for producing a compound represented by general formula (1) as represented by the following formula (where the symbols in the formula are the same as defined in the specification) or a salt thereof, wherein a compound represented by general formula (2) is produced, a pyrazole ring being formed via a reaction between a compound represented by general formula (3) and phosphorus pentasulfide; and, once the compound represented by general formula (2) is deprotected, a carboxylate of a compound represented by general formula (6) is produced, the compound obtained by forming a carboxylic acid and a salt.
WO2008106633A1 Methods of using benzodioxine compounds in treating sodium channel-mediated diseases or conditions This invention is directed to compounds of formula (I): wherein n, m, X, Y, Q, R1, R2, R3, R4, R5, R6 and R7 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, and their use for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
CN102863397A Quinoxaline keto-amide compound, preparation method and application thereof The invention discloses a quinoxaline keto-amide compound. The structural general formula is represented as follows, wherein R1 represents a methoxy group or hydrogen, and R represents hydrogen or halogen. The invention further discloses a preparation method of the quinoxaline keto-amide compound and an application of the quinoxaline keto-amide compound in preparing anti-tumor angiogenesis drugs. According to the quinoxaline keto-amide compound, by means of activity evaluation of in-vitro cellular levels and organization levels, angiogenesis of new vessels can be effectively inhibited, and a methyl thiazolyl tetrazolium (MTT) experiment proves that obvious cytotoxicity is absent so that the quinoxaline keto-amide compound can be used as a novel anti-tumor angiogenesis inhibitor, wherein anti-angiogenesis activity of three compounds (SLL-4, SLL-7 and SLL-16) is superior to that of pazopanib of a positive control drug, and a further in-vitro screening result can preliminarily show that the three quinoxaline keto-amide compounds can be expected to be candidate drugs. In a word, a quinoxaline ketone framework is promising to be used for designing and synthesizing the novel anti-tumor angiogenesis inhibitor.
WO2007039057A1 Cosmetic compositions comprising hydroxyfatty acids The present invention is concerned with novel cosmetic or pharmaceutical compositions. More particularly, the invention is concerned with novel cosmetic or pharmaceutical compositions for treating or preventing any symptoms caused by negative developments of the physiological homeostasis of healthy skin, as well as for the promotion of hair growth and protection from hair loss.
US20100144657 PHENYLPIPERIDINE MODULATORS OF mu-OPIOID RECEPTORS The present invention relates to new phenylpiperidine modulators of opioid μ-receptors, pharmaceutical compositions thereof, and methods of use thereof.
CA2340343C Enantioselective synthesis A short practical commercial process for the efficient enantioselective synthesis of the non-steroidal antiestrogen of formula (I) or (XIV) or a pharmaceutically acceptable salt thereof.
CN102755428A Calculus bovis yijin tablet for treating chronic pharyngitis and preparation method thereof The invention discloses a calculus bovis yijin tablet for treating chronic pharyngitis. The calculus bovis yijin tablet for treating chronic pharyngitis comprises the following raw materials by part of weight: 150-250 parts of golden cypress, 80-120 parts of honeysuckle, 70-120 parts of platycodon grandiflorum, 50-80 parts of blackberry lily, 1-4 parts of menthol crystal and 1-4 parts of calculus bovis. The invention further discloses a preparation method of the calculus bovis yijin tablet. The preparation method is simple in preparation, the obtained medicine can clear heat to decrease internal heat, clear away intense heat and toxic substances, dissolve phlegm, scatter wind heat, diffuse lung qi, relieve sore throat, eliminate phlegm and pus and cure pharyngitis and pharyngalgia, radically solves the problem of aetiological agent of chronic pharyngitis, directly removes nidus, achieves the aim of treating both principal and secondary aspects of diseases, and is good in curing effect and chronic pharyngitis is not apt to reappear.
WO2007034748A1 Immunomodulating agent in gut Discloses is an immunomodulating agent in the gut, which can be ingested continuously in the daily dietary habit and does not produce any adverse side effect. The immunomodulating agent comprises a cyclic tetrasaccharide as an active ingredient.
WO2011132075A3 A hydrate of a cyclohexanamine derivative This invention provides a cyclohexanamine derivative which is useful as a medicine. It was found that a hydrate of a cyclohexanamine derivative is useful as an active pharmaceutical ingredient.
US20090176880 Methods for Culturing Human Lung Mast Cells and Uses Thereof Methods for culturing human lung mast cells in the absence of co-culture with feeder cells which are viable for longer than 4 days are provided. Also provided are methods for using these human lung mast cell cultures to assess biological and pharmacological activities of these cells in vivo and to identify modulators of the survival, proliferation, function and phenotypic expression of human lung mast cells. Modulators identified via these cells are useful in the prevention and treatment of diseases involving human lung mast cell function.
EP1397135B1 Combination of a pde4 inhibitor and tiotropium or derivative thereof for treating obstructive airways The present invention relates to a combination of therapeutic agents useful in the treatment of obstructive airways and other inflammatory diseases comprising (I) a PDEIV inhibitor that is therapeutically effective in the treatment of said diseases when administered by inhalation; together with (II) an anti-cholinergic agent comprising a member selected from the group consisting of tiotropium and derivatives thereof that is therapeutically effective in the treatment of said diseases when administered by inhalation; as well as to a method of treating said obstructive airways and other inflammatory diseases comprising administering to said mammal by inhalation a therapeutically effective amount of said combination of therapeutic agents; and a pharmaceutical composition comprising a pharmaceutically acceptable carrier together with said combination of therapeutic agents; and a package containing a pharmaceutical composition for insertion into a device capable of simultaneous or sequential delivery of said pharmaceutical composition in the form of an aerosol or dry powder dispersion to said mammal, where said device is a metered dose inhaler or a dry powder inhaler. It is preferred that said anti-cholinergic agent component be tiotropium bromide.
CN102442986A Application of natural compound P61 in inhibition of reproductive growth of tumor cells The invention discloses a natural compound P61 capable of inhibiting the reproductive growth activity of tumor cells and an application thereof. The structural formula of the natural compound P61 is shown in a formula I. The compound or its pharmaceutically acceptable salt can be used for preparing medicines capable of inhibiting the proliferation of eukaryotic tumor cells or medicines capable of preventing and/or treating tumor. The in vitro antitumor test confirms that the compound P61 has good inhibition effects for breast cancer cell (MCF-7), lung cancer cell (A549), ovarian cancer cell (SKOV3), colorectal cancer cells (Caco2, SW480) and vero fibroblast (COS-7).
WO2014142520A1 Phenyl carbamate compounds for use in preventing or treating epilepsy or epilepsy-related syndrome The present invention provides a pharmaceutical composition for preventing and/or treating a epilepsy or epilepsy-related syndrome, for example an intractable epilepsy or its related syndrome such as drug-resistant epilepsy, comprising the phenyl carbamate compound as an active ingredient, and a use of the phenyl carbamate compound for preventing and/or treating epilepsy or epilepsy-related syndrome.
US7622490 Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7 cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR9-S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7 cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
EP2608781A1 Inclusion complexes of cyclodextrins with spermidine, and proliferative/reparative compositions comprising thereof The invention refers to inclusion complexes formed by cyclodextrins with spermidine with a molar ratio ranging from 1 : 1 to 1: 10 mol/mol, preferably 1:2 mol/mol, which have a significantly enhanced proliferative/mitotic effect on fibroblasts. It further refers to medicinal/cosmetic compositions comprising said inclusion complexes for the maintenance and repair of damaged or senescent connective tissues and mucosa.
EP2427192A1 Use of osi-906 for treating adrenocortical carcinoma A method of treating adrenocortical carcinoma with OSI-906.
WO2013023339A1 Secologanolic acid, pharmaceutical composition comprising same and use thereof A secologanolic acid used as a preventive agent and/or a therapeutic agent for diseases caused by bacteria. The secologanolic acid can resist various multiple antibiotic resistant bacteria including multidrug-resistant grampositive bacteria and gramnegative bacteria; and can be used in the preparation of drugs for the prevention and/or treatment of diseases caused by bacteria, especially multiple antibiotic resistant bacteria. Pharmaceutical compositions comprising secologanolic acid are included. A method for the prevention and/or treatment of diseases caused by bacteria, comprising the administration of a therapeutically effective amount of secologanolic acid and/or a pharmaceutical composition thereof to patients in need thereof.
CN1903869A Tibifudine derivative salt and its preparation method and pharmaceutical application The present invention relates to metal salt derivative of tibifdine, in particular, it relates to sodium salt and potassium salt derivative of tibifdine and its hydrate. Besides, said invention also provides a method for preparing metal salt derivative of tibifdine and its hydrate, and also provides preparation composition containing metal salt derivative of tibifdine or its hydrate, its preparation method and medicine application.
US20100124537 Medical applications of alpha-ketoglutarate The invention relates to a new use of alpha-ketoglutarate for manufacturing of medical preparation for prophylaxis or treatment of undesired medical conditions associated with the presence and/or activity of ureolytic bacteria in living organisms, except plants, including a human being, pet and farm animal, such as mammal, bird, amphibian, fish, molluse or arthropod, whereas the undesired medical conditions is a condition associated with the presence and/or activity in the gastrointestinal tract, respiratory and/or urogenital system of ureolytic bacteria from the group including Helicobacter pylori, bacterial strains from the Brucella genus, urease-positive bacteria such as Ureaplasma ureolyticum and other alkalophilic bacteria, such as for instance Bacillus pasteurii, urease-producing Yersinia enterocolica rods, ureolytic bacteria that participate in the formation of biofilm and mineralisation of deposits on catheters and other medical equipment, ureolytic bacteria causing infections of the mucous membrane in the oral cavity, gingival diseases, dental caries, causing formation of tartar, ureolytic bacteria responsible for formation of infectious stones in course of urinary system infections of the genii: Proteus, Ureaplasma, Klebsiella, Pseudomonas, Staphylococcus, Providencia, Corynebacterium, in particular P. mirabilis, and mycoplasmas causing genital tract—in particular its lower part infections, Mycoplasma hominis and U. urealyticum. The invention also covers new medical preparations, dietary supplements, special medicated food and food/feed additives containing alpha-ketoglutarate, useful in prophylaxis and inhibition of colonisation of living organisms, except plants, including a human being, pet and farm animal, such as mammal, bird, amphibian, fish, molluse or arthropod, by harmful ureolytic bacteria, in particular organisms of human beings and domestic animals by H. pylori. Moreover, according to the invention alpha-ketoglutarate is used as an active ingredient in methods of prophylaxis and treatment of the a.m. diseases and conditions associated with ureolytic bacteria, as well as in a process for the manufacture of organic biofuel, based on the conversion of biomass comprising of lignin and cellulose by means of bacterial enzymes, wherein the enzymes produced by hindgut ureolytic microbiota of wood-feeing higher termites are used in presence of alpha-ketoglutarate.
CN101906119A Novel method for preparing tenofovir The invention relates to a novel method for preparing tenofovir, in particular to a method for preparing a tenofovir compound, in particular the monohydrate of the tenofovir for resisting hepatitis B viruses and human immunodeficiency viruses. The method comprises the following steps of: using (substituted) triphenylchloromethane XIII to protect hydroxy in the end position of (R)-1,2-propanediol,condensing the obtained product with dialkyl sulfonyloxy methyl phosphonate V to obtain XV, hydrolyzing the XV in the aqueous solution of an organic acid to remove the protective group of the hydroxyl at the end position of XV to obtain an intermediate XI, condensing sulfonate XII of the intermediate XI with adenine to obtain an intermediate VII, transforming the intermediate VII into the corresponding trimethylsilyl phosphonate VIII by trimethylsilyl bromide (TMSBr), and hydrolyzing the VIII to obtain the target product. The method has the advantages of short process route, convenient operation, low cost and easy access of raw materials and favorability for large scale production.
WO2009077497A2 Azolyl methyl oxiranes, the use thereof, and agents containing them The present invention relates to azolyl methyl oxiranes of the formula (I), wherein the variables A, B, and D have the meanings as defined in the description and the claims.
WO2008127594A2 Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.
US20100196501 Silver-containing foam structure A method of producing a hydrophilic polyurethane foam structure containing a silver salt, chosen from the group of silver sulphate, silver citrate, silver acetate, silver carbonate, silver lactate and silver phosphate, or a mixture of these salts includes the steps of (a) providing a water phase containing a surfactant, and at least one silver salt, wherein the at least one silver salt is dispersed in the water phase; (b) providing a isocyanate-terminated polyether having functionality of more than (2); (c) mixing the water phase and the isocyanate-terminated polyether, immediately transferring the resulting mixture to a mould whereby a foam structure is obtained; and (d) drying the foam structure until it has a moisture content of at most 10% (wt). The hydrophilic polyurethane foam structure produced by the method and a wound dressing containing the foam structure are also described.
EP1517707A1 Treatment for depression and anxiety with the combination of a pde iv inhibitor and an antidepressant or an anxiolytic agent The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a PDE IV inhibitor in combination with an antidepressant or an anxiolytic agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a PDE IV inhibitor and an anxiolytic agent or antidepressant.
WO2006090768A1 Process for production of optically active ppar-activating compound and intermediate of the same A process for producing a compound (4) comprising the step of reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1) comprising the step of reacting a compound (2) with a compound (3) in the presence of a base to yield a compound (4) and then deesterifying the compound (4) to yield the compound (1). These processes can produce a compound (1) and an intermediate thereof in high yield and high optical yield.
CN1660851A Ramification of water-soluble camptothecin and preparation method A water-soluble camptothecine derivative, its pharmacologically acceptable salt, its preparing process, and its application in treating tumor are disclosed.
US20080089838 antibody binds target tissue and conjugate carrying epitope (haptens); monoclonal antibody or fragment thereof binds to a colon-specific antigen-p mucin (CSAp) antigen - the Mu-9 epitope; DNA sequence; anticancer The present invention provides humanized, chimeric and human anti-CSAp antibodies and anti-CSAp antibody fusion proteins that are useful for the treatment and diagnosis of various cancers, including colon cancer.
CN101322722A Compound carbamylcholine chloride injection for animals and preparation method thereof The invention discloses an veterinary compound bethanechol chloride injection and a preparation method thereof and aims at providing a compound bethanechol chloride injection which can quickly take effect on constipation of livestock, relieve the stress reaction of the bodies of the ill livestock, and treat constipation both from the superficiality and origin and a preparation method with simple process and easy realization. Every 100L of the injection is composed of the following components: 0.05-0.4kg of bethanechol chloride, 10-50kg of bile, 20-100kg of 95% ethanol, 0.5kg of Tween 80, 2kg of talc powder, 0.2kg of sodium bisulphite, 0.01kg of EDTA-2 Na, and sufficient water for injection. The invention is a compound preparation of bethanechol chloride for stimulating the intestinal motion of the livestock and the bile with the function of removing heat and toxic materials, which has double efficacies, reasonable formula and reasonable determination of contents of components, quickly takes effect on treating constipation of livestock, and treats constipation both from the superficiality and origin. The injection has the advantages of preventing the abnormal fermentation of the gastrointestinal feed chyme, and improving the curative ratio.
CN103142589A Mezlocillin sodium pharmaceutical composition for injection and preparation method thereof The invention provides a mezlocillin sodium pharmaceutical composition for injection and a preparation method thereof, relating to the field of a medicinal preparation and a preparation method thereof. The invention mainly solves the problems of high dosage of single mezlocillin sodium and metronidazole preparation, poor treatment effect after combination, and great side effect in the prior art. The pharmaceutical composition comprises mezlocillin sodium and metronidazole lipid microspheres in a weight ratio of 100:3-100:10, wherein the weight of the metronidazole lipid microspheres is metered on the basis of metronidazole; and when the pharmaceutical composition is prepared into a freeze-dried powder injection, the pH value of the water solution of the pharmaceutical composition is 6.5-7.0. The pharmaceutical composition freeze-dried powder injection provided by the invention has high curative effect, and can reduce the consumption of the metronidazole by more than 80%, thereby greatly relieving or avoiding the toxic and side effects of the metronidazole, especially digestive tract reactions, including nausea, vomit, inappetence, abdominal colic and neurotoxicity, and lowering the incidence rate of adverse reactions.
US20110054029 Water-soluble dietary fatty acids Water-soluble dietary fatty acid formulations, solutions, and methods for increasing the water solubility and/or bioavailability of dietary fatty acids, as well as methods for treating various diseases are disclosed.
CN102648913A External compound preparation composition for resisting skin itch The invention discloses an external compound preparation composition for resisting skin itch. The external compound preparation composition comprises the following components: (a) lidocaine hydrochloride, (b) cetirizine hydrochloride or a laevo isomer thereof and (c) conventional medicinal auxiliary materials, wherein the weight ratio of the lidocaine hydrochloride to the cetirizine hydrochloride is 1:1-10:1; and the weight ratio of the lidocaine hydrochloride to the levocetirizine dihydrochloride is 2:1-20:1. In the external compound preparation composition disclosed by the invention, the histamine H1 receptor blocking action of an antihistamine medicament, i.e., the cetirizine hydrochloride and the nerve conduction retarding action of a local anesthetic, i.e., the lidocaine hydrochloride are utilized fully, so that the skin itch resistance is improved; moreover, corticosteroids is not contained, so that side effects are reduced, and the compliance of a patient is improved; and discovered by pharmacodynamics study, the external compound preparation composition has a good synergic action, and can be applied to treatment of skin itch caused by a plurality of factors.
CN102579471B Applications of four gypenoside compounds in preparation of medicament for treating tumors The invention relates to a gynostemma pentaphyllum leaf extract which is rich in damulin A, damulin b, gypenoside L and gypenoside LI, and applications of four saponin compounds to preparation of a medicament for treating tumors. Cancers are selected from lung cancer, stomach cancer, liver cancer, breast cancer or leukemia.
WO2010142779A1 Antifungal 1,2,4-triazolyl derivatives having a 5- sulfur substituent The present invention relates to novel triazole compounds of the formulae (I) and (Il) as defined below, to agricultural and pharmaceutical compositions containing them and to their use as fungicides antiviral and anticancer agents.
US20070244030 Method for Assessing Cancerous State The present invention relates to a method for assessing a cancerous state of a mammal-derived specimen, which comprises: (1) a first step of measuring a methylation frequency of Neurofilament3 gene contained in a mammal-derived specimen or an index value having the correlation therewith, and (2) a second step of determining a cancerous state of the specimen based on a difference obtained by comparing the measured methylation frequency or the index value having the correlation therewith, with a control; and the like.
WO2014006130A1 IMIDAZO[2,1-b]THIAZOLE DERIVATIVES, THEIR PREPARATION AND USE AS MEDICAMENTS The present invention relates to new imidazo[2,1-b]thiazole derivatives (I) having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
CN102764269A Nasal cavity health care cleansing solution and preparation method thereof The invention discloses a nasal cavity health care cleansing solution and a preparation method thereof. The cleansing solution is characterized by comprising, by mass, 1-15 parts of salt, 0.5-10 parts of L-aspartate, 0.2-5 parts of iron lactate, 0.3-8 parts of magnesium citrate, 0.2-5 parts of zinc gluconate, 0.01-0.5 part of sodium selenite, 2-10 parts of glycerol, 3-20 parts of potassium citrate and 100-300 parts of water. By means of the mass fraction of components of the nasal cavity health care cleansing solution, the preparation method includes the process of A, adding water into the salt, the L-aspartate, the iron lactate, the magnesium citrate, the zinc gluconate and the sodium selenite for dissolution to obtain an A solution; B, adding water into the glycerol and the potassium citrate for dissolution to obtain a B solution; and C, slowly adding the A solution into the B solution, continuously stirring the solution until the solution is clarified, performing standing reaction for 5-10 hours and filtering and deslagging the solution to obtain the nasal cavity health care cleansing solution.
US7375116 NMDA (N-methyl-D-aspartate) receptors; eg 6-(4-benzylpiperidin-1-carbonyl)-1,5-dihydro-oxazolo[4,5-f]indole-2-one Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
US20110294806 Azaindole derivatives as kinase inhibitors This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
CN101703753B Medicinal composition powders or granules for treating whitevein and preparation method thereof The invention discloses a medicinal composition powders or granules for treating whitevein and a preparation method thereof. The powders or granules are prepared by taking a formula of conventional Tibetan medicament white-plus unguent as a basic formula and modifying the formulation. In the invention, an adopted preparation method of extracting some medicinal materials and making other medicinalmaterials into superfine powder effectively retains the active ingredients in the medicinal materials, greatly improves the raw medicament component content and improves bioavailability, so that the curative effect of the gel is better. The powders or granules of the invention adopt a medicated bath therapy which is favorable for the absorption of medicaments and increases the effect of a medicament therapy. The method for preparing the medicinal composition powders or granules is easy and feasible, and is easy for industrialization.
US20130224256 Hydrogel nanocomposite wound dressing and a method of synthesizing the same The various embodiments herein provide hydrogel nanocomposite wound dressing comprising a polymeric basal matrix, a reinforcing agent, a biological sensor and an antibiotic for a slow release in a wound when applied. The polymeric basal matrix is made up of polyvinyl alcohol polymer with an amount of 1-15% by weight. The reinforcing agent comprises clay nanoparticles to inhibit a sudden drug release. The clay nanoparticles comprise montmorillonite nano particles with an amount of 0-2% by weight. The biological sensor is a peptide chain. The peptide chain is thrombin sensitive with an amount from 50 to 200 mg. The antibiotic is gentamycine with an amount of 1-3% by weight. The embodiments herein also provide a method of synthesizing the hydrogel nanocomposite wound dressing.
US8252306 Process for preparing a semi-solid delivery vehicle comprising granisetron A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.
US20090118376 Memantine Protects Inflammation-Related Degeneration of Dopamine Neurons Through Inhibition of Over-Activated Microglia and Release of Neurotrophic Factors from Astroglia This invention discloses that memantine (MMT) protects dopamine (DA) neurons damage through its potent anti-inflammatory effect by inhibiting microglial over-activation and the protection on DA neuron is a dose-dependent response. This invention also discloses that NADPH oxidase plays a critical role of neuroprotection of MMT and MMT therapy for neurodegeneration diseases acts in part through an alternative novel mechanism by reducing microglia-associated inflammation. In addition, this invention reveals that MMT is neurotrophic to DA neurons through the release of neurotrophic factors from astroglia.
CN1985835A Prepnaring method for freeze dried tigecycline powder for injection The present invention relates to preparation process of freeze dried tigecycline powder for injection. The preparation process includes the following steps: introducing clean treated air into water for injection at 5-30deg.c to replace its oxygen, adding tigecycline through stirring for dissolving, adding active carbon for injection in 0.1 g/100ml while further introducing clean air and stirring for 15-30 min, coarse filtering to eliminate active carbon, filtering with 0.45 micron microporous membrane, introducing clean air into the filtrate, filtering with 0.22 micron microporous membrane, packing in 5-15 ml size antibiotic ampoule, pre-freezing for 3-6 hr, freeze drying for 24-48 hr, covering, and rolling aluminum cap. The present invention has raised clinical safety.
WO2014096196A1 An oral iron (iii) based phosphate adsorbent for treating iron-deficiency anemia in cats with chronic kidney disease The invention relates to the new use of an oral iron(III)-based phosphate adsorbent, for example SBR759, in the treatment of iron deficiency anaemia in cats with chronic kidney disease.
CN101006994A Enteric-coated capsules of allimin and its preparation method The invention relates to a kind of allicin capsulate enterosolubilis as well as its preparing method. The invention is composed by garlic oil, beta-schardinger dextrin and starches. The preparing procedure includes the following steps: putting purified water and beta-schardinger into the castration jar in turns and heating them; stirring to get the emulsified suspension; putting garlic oil into the jar and keeping stirring at a certain temperature for several hours; pumping the mentioned materials into the storage tank, stetting at low temperature; removing water through filtering; after heating, airblast drying, pulverizing and sieving the materials, mixing them with starches; getting the particles or micro pallets with 75% as the demulcent; cryodrying; polishing; loading the materials into the No. 1 capsulae enterosolubilis; packaging. The invention belongs to hard capsule dosage form; it's capsulae enterosolubilis (white or off-white color particles); its specification is 20mg/grain. The advantages of the invention includes: up-to-date idea, proper design, standard technology, simple preparing method, easily available medicine, low cost, convenient to take with, easy absorption by intestinal tract, no gastric irritation, excellent curative effect, good acceptability, no pollution and it's easy to realize production in quantity. The product is applicable to prevent and treat deep part fungus infection such as bellows and alimentary canal fungus infection; blastomyces alb cans bacteria, chronic and acute enteritis, whooping cough and so on.
US20090118280 schizophrenia; 1-[4-(4-morpholinylcarbonyl)phenyl]-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazole; administered alone or with another antipsychotic drug Compounds of formula (I) and salts are provided: along with pharmaceutical compositions, uses in medicine, e.g., treating disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment.
CN102766148A Cefamandole nafate compound and composite thereof The invention relates to a cefamandole nafate compound and a composite thereof. The cefamandole nafate compound is detected by using a powder X-ray diffraction method, and an X-ray powder diffraction pattern indicated by a diffraction angle at 2 theta +-0.2 degrees shows characteristic diffraction peaks at 11.45 degrees, 13.63 degrees, 14.68 degrees, 15.69 degrees, 18.39 degrees, 20.30 degrees, 26.09 degrees, 27.11 degrees, 28.74 degrees, 30.27 degrees, 31.90 degrees, 34.01 degrees and 35.88 degrees. The cefamandole nafate compound and a preparation of the cefamandole nafate compound have good stability, and therefore curative effect of the preparation is improved, and effectiveness and safety of drugs are guaranteed.
CA2223503C Transferrin receptor genes Purified and isolated nucleic acid is provided which encodes a transferrin receptor protein of a strain of Haemophilus or a fragment or an analog of the transferrin receptor protein. The nucleic acid sequence may be used to produce peptides free of contaminants derived from bacteria normally containing the Tbp1 or Tbp2 proteins for purposes of diagnostics and medical treatment. Furthermore, the nucleic acid molecule may be used in the diagnosis of infection. Also provided are recombinant Tbp1 or Tbp2 and methods for purification of the same. Live vectors expressing epitopes of transferrin receptor protein for vaccination are provided.
WO2008096829A1 Tricyclic compounds PPARϜ agonists containing tricyclic compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof as the active ingredient, wherein R1 is optionally substituted lower alkyl or the like; R2 and R3 may be the same or different and are each optionally substituted lower alkyl or the like; R4 and R5 may be the same or different and are each hydrogen or the like; Q1-Q2-Q3 is CH=CH-CH=CH or the like; Y is a single bond or the like; Z1-Z2 is C=CR13 or the like wherein R13 is hydrogen or the like; and A is -COOH or the like.
EP2628798A1 Prophylactic or therapeutic agent for fibrosis Provided is siRNA effective for the treatment of fibrosis and a pharmaceutical containing the siRNA. An siRNA having a full length of 30 or fewer nucleotides and targeting a sequence consisting of 17 to 23 consecutive bases selected from the group consisting of bases at positions 1285 to 1318, bases at positions 1398 to 1418, bases at positions 1434 to 1463, bases at positions 1548 to 1579, bases at positions 1608 to 1628, bases at positions 1700 to 1726, bases at positions 1778 to 1798, bases at positions 1806 to 1826, and bases at positions 1887 to 1907 of SEQ ID NO: 1.
US20120135048 novel formulation of indomethacin The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.
US20070270357 Bifunctional Macrolide Heterocyclic Compounds and Methods of Making and Using the Same The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of bifunctional compounds useful as therapeutic agents. These compounds have both a macrolide ring and at least one heterocyclic moiety. The present invention further relates to processes for the preparation of such compounds, to intermediates useful in their preparation, to the use of the compounds as therapeutic agents, and to pharmaceuticals compositions containing them.
WO2007067490A1 POLYMORPHS OF ANDROGEN RECEPTOR MODULATOR - (N-3H-IMIDAZO [4 , 5-B] PYRIDIN-2-YL-METHYL) -2-FLUORO-4-METHYL-3-OXO-4-AZA-ANDROST- l-EN-17 . BETA . -CARBOXAMIDE Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer’s disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
US7766013 Aerosol generating method and device A method and device are provided to generate an aerosol having a desired particle sizes, i.e., from molecular to about 10 microns, which can be used to effectively deliver a physiologically active compound to organs and tissues such as the lung, eye, mucosa and skin. The aerosol is formed through vaporization of the compound while mixing the resulting vapor with a gas, in a ratio, to form the desired particle size when a stable concentration of particles in the gas is reached.
CN101485652B Composition of taxone compound, and preparation method and application thereof The invention discloses a drug composition of taxanes, which comprises taxane compounds with effective dosage for treatment, a surfactant, a cosolvent and a stabilizer, wherein the cosolvent is selected from one or a mixture of more of polyethylene glycol, propylene glycol, glycerine or ethylene glycol; and the stabilizer is selected from hydrochloride, carbonate, phosphate and nitrate or a mixture of hydrochloride, carbonate, phosphate and nitrate. The composition can be an injection, a frozen dry powder needle or a kit for combined use. The composition can improve the solubility and stability of the taxane compounds. The invention also discloses a method for preparing the drug composition and application of the drug composition.
WO2013134288A1 Polymorphic forms of (s)-2-(1-(9h-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3h)-one Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin- 4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed.
CN103251951A Application of P2X2 receptor agonist or opening agent in preparation of anti-depression or anti-anxiety drugs The invention discloses an application of a P2X2 receptor agonist or a P2X2 receptor opening agent in preparation of anti-depression or anti-anxiety drugs. According to the present invention, experiment research results confirm that: the P2X2 receptor agonist or the P2X2 receptor opening agent has an anti-depression and/or anti-anxiety effect, such that the P2X2 receptor agonist or the P2X2 receptor opening agent can be used for preparing anti-depression or anti-anxiety drugs, and can be adopted to screen prevention and treatment target points of anti-depression and/or anti-anxiety drugs and screen early stage pre-warning and clinical diagnostic reagents of depression and/or anxiety so as to provide broad application prospects.
US7105547 N-{3-[3-fluoro-4-(4-oxo-3,4-dihydro-2H-pyridin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide; treating gram-negative organisms such as Haemophilus influenza and Moraxella catarrhalis. The present invention provides antibacterial agents of formula I, or a pharmaceutically acceptable salt thereof.
US7368471 fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis, Alzheimer's disease; {1-Methyl-6-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}(oxo)acetic acid This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
WO2008153182A1 Morpholine derivative Disclosed is a morpholine derivative represented by the formula [I] below, which is useful as a renin inhibitor, or a pharmacologically acceptable salt thereof. (In the formula, R1 represents (A) an alkyl group substituted with a group selected from optionally substituted alkoxy groups or the like, (B) an optionally substituted aryl group, (C) an optionally substituted heterocyclic group, (D) a cycloalkyl group or (E) an alkyl group; R2 represents (A) an alkyl group substituted with a group selected from optionally substituted alkoxy groups or the like, (B) an optionally substituted aryl group, (C) an optionally substituted heterocyclic group, (D) an optionally substituted alkylcarbonyl group, (E) an optionally substituted arylcarbonyl group, (F) an optionally substituted heterocyclic group-substituted carbonyl group or (G) a cycloalkylcarbonyl group; T represents a methylene group or a carbonyl group; and R3, R4, R5 and R6 may be the same or different, and each represents a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group.)
CN1593391A Application of biphenyl cyclooctene containing substance in the process for preparing Alzheimer disease treating medicine The invention discloses the application of biphenyl cyclooctene containing substance in the process for preparing Alzheimer disease treating medicine, wherein the substance has the formula disclosed in the specification. The biphenyl cyclooctene containing substance can effectively reduce the output of Abetta, suppress the formation of aged speckle, improve the learning and memory capability for the modeled mouse, thus achieving the goal of treating and delaying AD disease.
US20050129694 At least one (SEK) kinase inhibitor that acts in an synergistic manner to those inhibiting the virus multiplication for the Raf/MEK/ERK signal transmission path; influenza viricides The invention relates to the use of at least one active substance for producing a pharmaceutical composition for the prophylaxis and/or treatment of at least one viral disease. It is characterized by active substance(s) which inhibit(s) either at least two kinases or at least one SEK kinase of a cellular signal transmission path such that virus multiplication is inhibited.
US7883719 Pasting agent A patch comprising a backing layer and an adhesive layer disposed on the backing layer and compounded with an adhesive agent and oxybutynin and/or a pharmaceutically acceptable salt thereof, wherein the adhesive agent comprises an acrylic polymer substantially free of both carboxyl group and hydroxyl group and a rubber polymer, in which weight ratio of content of the acrylic polymer to content of the rubber polymer is from 1:4 to 1:19.
CN101313913A Hyaluronate lyase restrainer The invention relates to a hyaluronidase inhibitor containing new ingredients, and an anti-aging agent for skin and an anti-inflammatory agent which contain the hyaluronidase inhibitor. Active ingredients of the hyaluronidase inhibitor are phenylethanoid glycosides. The invention discloses that the hyaluronidase inhibitor has blocking activity against hyaluronidase, that is, the invention finds out that, in orobanchaceae, cistanche tubulosa has the highest content of phenylethanoid glycosides, and carries out purification for extracts of cistanche tubulosa for the first time to prepare phenylethanoid glycosides which are effective ingredients of the cistanche tubulosa. According to pharmacological experiments, the phenylethanoid glycosides have a notable effect on reinforcing memory and inhibiting the formation of a blood thrombus, etc.
WO2007133812A2 Improved carriers for delivery of nucleic acid agents to cells and tissues This invention relates to drug delivery and specifically to the preparation and use of functionalized carriers such as nanopolymers and nanovesicles for improved delivery of nucleic acid agents (NAA) to tissues and cells. These compounds have broad applicability for treating numerous diseases and disorders, including neurodegenerative and neuromuscular disorders. The concept encompasses preferably polymeric carriers for delivery of a class of oligonucleotides that modulate RNA splicing.
CN102188689B Compound combination medicament for treating COPD, preparation method and application thereof The invention discloses a compound combination medicament for treating COPD, a preparation method and an application thereof. The compound combination medicament comprises the following components by weight: 10 to 60 parts of codonopsis pilosula, 20 to 50 parts of rhubarb, 40 to 100 parts of root of scutellaria, 15 to 60 parts of lapis chlorite (fried), 10 to 60 parts of bighead atractylodes rhizome (fried), 20 to 60 parts of poria cocos, 10 to 100 parts of pinellia, 5 to 70 parts of reddish orange, 15 to 120 parts of ephedra, 10 to 110 parts of almond, 10 to 150 parts of agilawood, 10 to 60 parts of liguisticum chuanxiong, 5 to 160 parts of ginger, and 40 to 200 parts of earthworm. The compound combination medicament provided in the invention is used for treating the COPD at the attack stage and is mainly used for treating spleen-deficiency and lung-heat COPD, wherein the symptoms of the spleen-deficiency and lung-heat COPD are cough, asthma, expectoration with yellow or white mucoussputum, dry excrement, dry mouth, abdominal fullness and distension, flat tongue with tooth mark on it, thin and yellow tongue coating, and wiry and slippery pulse. The compound combination medicament provided in the invention is used for treating the COPD at the attack stage and is mainly used for treating spleen-deficiency and lung-heat COPD, wherein the symptoms of the spleen-deficiency and lung-heat COPD are cough, asthma, expectoration with yellow or white mucous sputum, dry excrement, dry mouth, abdominal fullness and distension, flat tongue with tooth mark on it, thin and yellow tonguecoating, and wiry and slippery pulse. The compound combination medicament has advantages of good curative effectiveness, short treating course, thorough treatment, no side effects and the like. Moreover, the compound combination medicament, which is made in a form of mixture, tablet, capsule, pellet, is easy to carry and to take.
WO2007082780A1 Use of alkanedicarboxylic acids and retinoids for treatment of rosacea and other inflammatory skin diseases In order to make available another therapeutic possibility for rosacea the use of at least one α,ω-n-alkanedicarboxylic acid with 7 to 13 carbon atoms or its esters and at least one retinoid for producing a pharmaceutical preparation is proposed. The suggested formulation is also effective in treatment of other inflammatory skin diseases such as psoriasis, atopic dermatitis and common acne.
WO2006038462A1 Novel steroid-producing cell [PROBLEMS] To provide a novel steroid-producing cell which is usable in treating abnormal steroid hormone secretion such as steroid hormone deficiency via transplantation or the like. [MEANS FOR SOLVING PROBLEMS] A steroid-producing cell characterized by having been differentiated from a bone marrow cell or a multipotent stem cell by transferring a factor participating in steroid hormone synthesis thereto is provided. Moreover, a method of producing this steroid hormone-producing cell, utilization thereof, a medicinal composition with the use of a hormone secreted by the cell and a method of treating various diseases by using the cell are provided.
CN102875565A Esterified podophyllum derivative with antitumor activity and preparation method and usage of esterified podophyllum derivative The invention discloses an esterified podophyllum derivative with antitumor activity and a preparation method and the usage of the esterified podophyllum derivative. The esterified podophyllum derivative with antitumor activity and shown as a formula (V) is obtained by means of esterification reaction of adamantine formic acid, orotic acid, 4-(pyrimidine sulfo) phenylacetic acid, cyclohexane carboxylic acid, 3,4-dimethoxy benzoic acid, 2-butoxycarbonyl-3-phenylalanine or 4-methoxy phenylacetic acid with podophyllotoxin or 4'-demethyl-epipodophyllotoxin. The esterified podophyllum derivative has multi-way multi-target actions on tumor cells to achieve better antitumor curative effects. According to in-vitro cell viability inhibition tests, the esterified podophyllum derivative has excellent antitumor activity and low toxic and side effects and can be prepared into antitumor drugs to be applied to antitumor treatment.
WO2013043719A1 Controlling appetite, promoting weight loss, reducing body fat, and/or improving glucose tolerance A method for treating obesity, insulin sensitivity, and related conditions involves administering to the subject a bacterium for overexpressing a N-acyl-phosphatidylethanolamine (NAPE) and/or a N-acylethanolamine (NAE). A composition includes a bacterium for overexpressing a N-acyl-phosphatidylethanolamine (NAPE) and/or a N-acylethanolamine (NAE); and an ingestible vehicle in which the bacterium is provided.
WO2007083985A1 Synergistic pharmaceutical composition of diclofenac and lysine clonixinate The present invention relates to the combination of two non-steroidal anti-inflammatory analgesic drugs: diclofenac, which has a predominantly anti-inflammatory action, and lysine clonixinate, which has a predominantly analgesic action. The combination is formulated in a single medicinal product in oral and injectable pharmaceutical forms. When the two drugs are combined in specific proportions, the combination produces pharmacological effects of analgesia, which indicate a superadditivity (synergy). The favourable profile of adverse effects observed after administration of the combination suggests that this therapeutic strategy may be a promising tool in the relief of moderate to severe acute pain.
US20080057068 SARMS and method of use thereof This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, muscle wasting diseases and/or disorders, bone-related diseases and/or disorders, diabetes, cardiovascular disease, renal disease and others.
US20090142310 Method of treating inflammatory arthropathies with suppressors of cpg oligonucleotides The present disclosure relates to oligodeoxynucleotides that suppress an immune response. Methods are disclosed for preventing or treating inflammatory arthropathies by administering a therapeutically effective amount of a suppressive oligodeoxynucleotide.
CN103142502A Calcitriol sustained-release granule and preparation method thereof The invention discloses a calcitriol sustained-release granule and a preparation method thereof. The calcitriol sustained-release granule disclosed by the invention consists of a quick-release granule core and a sustained-release coating layer, wherein the quick-release granule core consists of calcitriol and filler, and the sustained-release coating layer consists of a sustained-release material, a plasticizer, a pore-forming agent and an antisticking agent; and during preparation, the calcitriol sustained-release granule is obtained through coating the sustained-release coating layer outside the quick-release granule core. According to the calcitriol sustained-release granule and the preparation method of the calcitriol sustained-release granule, the drug is convenient in taking and slow in release, the aims of long acting and curative effect improving can be reached, and the dosage can be reduced while the same drug action is maintained, so that side effects to patients caused by drug taking are reduced; and the preparation method is simple, the quality of obtained products is stable, and thus, the method is applicable to large-scale production application.
EP1716123A1 Pyridazinone derivatives and their use as pde4 inhibitors Compounds of formula (1) are effective PDE4 inhibitors in which R1 is 1-4C-alkyl and R2 is 1-4C-alkyl, R3 represents a phenyl dervative of formulae (a) or (b) wherein R4 is 1-4C-alkoxy or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R5 is 1-8C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R6 is 1-4C-alkoxy, 3-5C-cycloalkoxy, 3-5C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R7 is 1-4C-alkyl and R8 is hydrogen or 1-4C-alkyl, or wherein R7 and R8 together and with inclusion of the two carbon atoms, to which they are bonded, form a spiro-linked 5-, 6- or 7-membered hydrocarbon ring, optionally interrupted by an oxygen or sulphur atom and R9 is hydroxyl, halogen, nitro, cyano, 1-4C-alkyl, trifluoromethyl, 1-4C-alkoxy, 1-4C-alkoxy which is completely or predominantly substituted by fluorine, hydroxycarbonyl, hydroxycarbonyl-1-4C-alkyl, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonylamino, 1-4C-alkylcarbonyloxy, 1-4C-alkylsulfonyl, benzyloxy, -C(O)R10, -S(O)2-R11, -O(CH2)n-C(O)-R12, -(CH2), -C(O)-R26 or -N(R29)R30.
EP2305274A1 Use of WNT stimulators for treating demyelinating diseases The present invention relates to the use of an effective amount of a Wnt, a Wnt-like substance, and/or a compound stimulating the Wnt signalling pathway for the preparation of a pharmaceutical composition intended to reduce the extent or degree of nerve demyelination in the central and peripheric nervous system of an individual suffering from a demyelinating disorder.
US20110251281 Composite Material Comprising High-Molecular-Weight Matrix and Low-Molecular-Weight Organic Compound and Process For Producing Same Previously reported composite materials comprising a hydrophilic high-molecular-weight matrix and a low-molecular-weight organic compound involve a problem in that: it is difficult to compound a high load of the low-molecular-weight organic compound in the high-molecular-weight matrix; and thus produced composite material yields a high-molecular-weight matrix component that can form a thrombus when contacting with blood. Now, it becomes possible to produce a composite material having an antithrombogenic activity and a high content of a low-molecular-weight organic compound by the present invention comprising the steps of: crosslinking a polymer with an organic acid derivative which is used as a crosslinker in an organic solvent while at the same time embedding the low-molecular-weight organic compound therein; and substituting the organic solvent by water after the production of the high-molecular-weight matrix to effect precipitation and compounding of the low-molecular-weight organic compound in the high-molecular-weight matrix.
EP1870411A1 Process for the preparation and purification of valgancyclovir A process for the preparation of valgancyclovir which comprises: a) reacting a compound of formula 7, in an aprotic solvent, in the presence of a condensing agent, with a compound of formula 8, wherein R1, and R2 may be, each independently, hydrogen, an halogen atom or an hydroxyl group; the double bond may either be in the E or Z configuration or a mixture thereof to yield a compound of formula 9 b) mild hydrolysis of compound obtained in a) to give valgancyclovir.
EP1351961B1 Substituted indolines as 5-ht receptor ligands The present invention provides pharmaceutically active compounds of formula (I) as described herein useful for the treatment of diseases or disorders of the central nervous system.
EP2014181A2 Compositions based on prebiotic and immunogenic ingredients for the prevention and treatment of gastroenteric disorders caused by dysbiosis and/or alterations of the normal intestinal flora The present invention relates to compositions containing bifidogenic and lactogenic prebiotic ingredients and immunogenic ingredients able to promote the proliferation and colonisation of bifidobacteria and lactic acid bacteria in the intestine, for the prevention and treatment of gastroenteric disorders.
CN101199798A Pressurized spray for treating rheumatism ache The invention discloses a spray for treating rheumatalgia. The spray is prepared by raw materials, namely, Oleum terebinthinae, Radix Angelicae Sinensis, Rhizoma Chuanxiong, Flos Carthami, Radix Saposhnikoviae, Radix Angelicae Pubescentis, Notopterygium incisum, Viscum album, Sanguis Draconis, Radix Angelicae Dahuricae, Asarum sieboldii, Carica Papaya, borneol, camphor, Artemisia lactiflora Wallex DC, Herba Abri, Leaf of argyi wormwood, Cortex Cinnamomi Cassiae, Pericarpium Zanthoxyli, Radix Achyranthis Bidentatae, Harms Manyprickle Acanthopanax, Caulis Piperis Kadsurae, Bungarus Parvus, Zaocys dhumnades, Semen Brassicae, Fructus Evodiae, rhizoma atractylodis, Milkvetch Root and Rhizoma Atractylodis Macrocephatae, which are all mixed in the proportion 1 : 1 and then brewed in yellow wine 1-10 times quantity of the total mixed drugs or sorghum liquor with more then 60 degrees for ten days. The invention has the efficacies of expelling rheumatism, dispelling cold-evil, promoting blood circulation by removing blood stasis, removing swelling and relieving pain, nourishing the stomach and invigorating the spleen, reinforcing the kidney and strengthening the bones, dredging meridians and collaterals and freeing channels, supplementing qi and nourishing blood, recovering and nourishing yin and strengthening antiviral ability and immunity of the human body.
CN102552175A Fludarabine phosphate lyophilized preparation for injection and preparation method thereof The invention discloses a fludarabine phosphate lyophilized preparation for injection and a preparation method of the lyophilized preparation, belonging to the technical field of medicament. The fludarabine phosphate lyophilized preparation is mainly prepared by active component of fludarabine phosphate and excipients; and the mass ratio of the fludarabine phosphate and the excipients is 1:0.5-2.0. Compared with the prior art, the fludarabine phosphate lyophilized preparation for injection has loose texture, rapidly dissolves in water and has good re-dissolving property; the lyophilized preparation is subjected to sublimation drying in vacuum, the water content is low, the stability is good, and long-term storage and clinical use of the products are facilitated; and besides, the preparation method of the preparation is simple, the transportation is convenient, and the production cost is effectively reduced.
US8324283 Solid pharmaceutical compositions comprising a SIP receptor agonist and a sugar alcohol A solid pharmaceutical composition suitable for oral administration, comprising: (a) a S1P receptor agonist; and (b) a sugar alcohol.
CN103373961A Preparation of (1, 3-diphenyl-1hydrogen-4-pyrazolyl) methyl benzoic acid serial compounds and applications in treatment of melanoma Provided are (1, 3-diphenyl-1hydrogen-4-pyrazolyl) methyl benzoic acid derivatives which are characterized by the following general formula:, wherein R1 can be 4-fluorine, chlorine, hydrogen, methyl and methoxy group, and R2 can be 4-fluorine, chlorine, hydrogen and methoxy group. The derivatives can inhibit multiplication of mouse melanoma A375 cell line, and so the derivatives can be used as potential anti-melanoma medicines. The invention discloses a preparation method for the compounds.
WO2011158933A1 Agent for treating renal fibrosis Provided is a carrier for delivering a substance to extracellular matrix-producing cells in the kidneys, the carrier containing a retinoid as the targeting agent. Also provided is an agent for treating renal fibrosis that uses the carrier. Further provided are methods for producing the carrier and the agent, production kits, and a method and the like for treating renal fibrosis using the same agent for treating renal fibrosis.
WO2014043296A1 Aminoisoquinoline derivatives as protein kinase inhibitors The present invention provides novel aminoisoquinoline compounds as defined in the specification, compositions thereof, use of these compounds as protein kinase inhibitors and as therapeutic agents for treatment of Raf kinase, in particular BRAFV600E kinase, related diseases or disorders, such as cancers. In addition, the invention also includes methods and processes for preparing these novel aminoisoquinoline compounds.
EP2441439A1 Pharmacological aid for prevention of incipient carious lesion and dentinal hypersensibility A pharmacological aid for prevention of incipient carious lesion and dentinal hypersensibility is disclosed, wherein said aid is a spray containing a liquid aqueous solution suitable to be sprayed in the patient's mouth. The aqueous solution comprises the following excipients: calendula, fluorides, hydroxylapatatite and thermo-gel agent suitable to transform said aqueous solution in gel, when the aqueous solution comes in contact with the patient's gums at a temperature of about 37 °C.
CN1951419A Capsule for treating cough, asthma and pharyngitis The invention discloses capsules for the treatment of common cold, cough, bronchitis, asthma, pulmonary emphysema, lung disease, phthisis, children's bronchitis, acute and chronic pharyngitis.
CN101366712B Method for preparing fat-soluble vitamin for injection The invention relates to a method for preparing fat soluble vitamins for injection. The fat soluble vitamins for injection contain vitamin A palmitate, vitamin D2, vitamin E, vitamin K1 and pharmaceutically acceptable supplementary materials. Sterile freeze-dried powder prepared by the fat soluble vitamins for injection through the low-pressure freeze-drying technology can simultaneously compensate all the four fat soluble vitamins through veins, and simultaneously can be dissolved in water-soluble diluent after special technological treatment, thus fat emulsion is not necessarily adopted as the diluent and the problem of inconvenience that the use of the fat soluble vitamins by patients is limited by the diluent is solved.
WO2010146585A4 Tellurium-containing compounds for treating viral infections Tellurium-containing compounds identified for use in a method of treating, or prophylaxis against, a viral infection caused by an influenza virus, uses thereof and pharmaceutical kits and pharmaceutical compositions comprising the same, are disclosed. The tellurium-containing compounds disclosed herein are suitable for co-administration with an antiviral agent.
US20090186883 Stable Aqueous Suspension An aqueous pharmaceutical suspension comprising: (i) at least one non-steroidal anti-inflammatory drug; (ii) an aqueous buffer system; (iii) xanthan gum; (iv) polyvinyl pyrrolidone; and (v) glycerol wherein the suspension is free from pregelatinised starch, amino polycarboxylic acid, microcrystalline cellulose, hydroxypropylmethyl cellulose, polyoxyethylene sorbitan monooleate, silicon dioxide and taste modifying agents selected from the group consisting of bulk sweeteners, intense sweeteners, flavouring agents and mixtures thereof.
US20080269325 Methods to Relieve Pain The invention is directed to a method of providing pain relief to a patient by administering to the patient an effective amount of a compound of Formula (I), which is represented by as RC(O)—NH—(CH2)n—CH═CH2, wherein R represents C1-20 alkyl, C2-20 alkenyl or C2-20 alkynyl; and n is an integer from 0 to 3.
US20100144836 Methods for Detecting Epigenetic Modifications A method of detecting a predisposition to, or the incidence of, cancer in a sample comprises detecting an epigenetic change in at least one gene selected from an NDRG4/NDRG2 subfamily gene, GATA4, OSMR, GATA5, SFRP1, ADAM23, JPH3, SFRP2, APC, MGMT, 11112, BNIP3, FOXE1, SYNE1, S0X17, PHACTR3 and JAM3, wherein detection of the epigenetic change is indicative of a predisposition to, or the incidence of, cancer. Also described are pharmacogenetic methods for determining suitable treatment regimens for cancer and methods for treating cancer patients, based around selection of the patients according to the methods of the invention. The present invention is also concerned with improved methods of collecting, processing and analyzing samples, in particular body fluid samples. These methods may be useful in diagnosing, staging or otherwise characterizing various diseases. The invention also relates to methods for identifying, diagnosing, staging or otherwise characterizing cancers, in particular gastrointestinal cancers such as colorectal cancers, gastric cancers and oesophageal cancers. The methods of the invention relate, inter alia, to isolating and analyzing the human DNA component from faecal samples and blood-based samples.
EP2307425A1 Imidazothiadiazoles derivatives Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.
US20090035302 Rage Antagonists As Agents To Reverse Amyloidosis And Diseases Associated Therewith Disclosed are RAGE antagonist compounds that have the ability to reverse pre-existing amyloidosis. Treatment with the RAGE antagonist compounds described herein may be used to reduce plaque size and improve cognition for subjects in the later stages of Alzheimer's disease. Additionally, the RAGE antagonists described herein may be used to reduce the onset of plaque formation and thereby prevent loss of cognition and other symptoms associated with Alzheimer's Disease and other diseases of amyloid deposition.
CN103705520A Method for preparing rivaroxaban solid composition The invention discloses a method for preparing a rivaroxaban solid composition. The method comprises the following steps: crushing rivaroxaban by adopting a wet crushing method, and simultaneously preparing a suspension solution; spraying the suspension solution into other auxiliaries to prepare grains with proper sizes; further preparing minimum medical dosage units. The method has the beneficial effects that: the problem that the grain diameter cannot be reduced to 5mu m when rivaroxaban particles are prepared by adopting a conventional crushing method can be solved, and the dissolution speed of the rivaroxaban preparation can be increased.
CN1954808A High dose Ambroxol hydrochloride freeze-dried preparation and preparation method A freeze-dried powder injection of high-dosage (500mg) ambroxol hydrochloride and its preparing process are disclosed.
CN101496796A Composite soft capsule of lycopene The invention relates to a lycopene compound soft capsule, which is prepared from lycopene, beta-carotene, vegetable oil, a stabilizer and proper capsule wall materials by a conventional preparation process. The lycopene compound soft capsule can remove free radicals in human body, improve the human immunity, beautify the face and remove the wrinkles, and keep the health of the skin.
CN101538230A Beta-amino ketones compound with anti-diabetic activity The invention discloses a beta-amino ketones compound with anti-diabetic activity, particularly the compound which has the general formula (I) as shown on the right or a pharmaceutically acceptable salt thereof. The invention can increase insulin sensitivity and/or decrease postprandial blood glucose level, and prevent and delay the outbreak and the development of diabetes mellitus and complications thereof, has simple preparation method, low cost and good potential application value and can be prepared to be anti-diabetic medicine for preventing and treating the diabetes mellitus.
EP2494965A2 Vitamin K for Prevention and Treatment of Skin Rash Secondary to Anti-EGFR Therapy The invention provides methods and compositions for treating and preventing a skin rash secondary to anti-epidermal growth factor receptor (EGFR) therapy, where the method comprises applying a vitamin K analog or a phosphatase inhibitor to the skin.
US20090227509 Modulation of hiv replication by rna interference Disclosed herein are small interfering RNAs (siRNAs), and vectors encoding one or more siRNAs (including short hairpin siRNAs), that are sufficiently homologous to a portion of the HIV genome to mediate RNA interference in vivo. Also disclosed are methods wherein siRNAs, or vectors encoding siRNAs, are administered to prevent or inhibit HIV infection in a subject, cell or tissue. Knockout and/or knockdown cells or organisms are also disclosed that utilize the siRNAs or vectors of the present invention.
WO2014141082A1 Agent for the prophylaxis and/or treatment of neoplastic diseases The invention relates to a novel agent in the form of rhodanine derivatives, which has prophylactic, antiproliferative and antimetastatic activity. Said agent can find use in medicine and pharmacology for the prophylaxis and/or treatment of neoplastic diseases of variable localisation.
US7510733 Epimerdinoside a oral pharmaceutics containing the same and preparatory and determination methods Epimeredinoside A extracted from Epimeredi indica root, oral pharmaceutics made up with the Epimeredi indica root extract and at least one pharmaceutical adjuvant, and preparatory method for the oral pharmaceutics. The root extract is the extracta sicca prepared by water extraction and concentration of Epimeredi indica root, and contains 0.10% to 1.50% of epimeredinoside A. The inventive pharmaceutics of Epimeredi indica root extract do not contain any hormone and progesterone is not needed to be taken to prevent a side effect after using the drug. The pharmaceutics has doubtless effect in treating female menopause.
US20100113474 Antineoplastic Combinations of 4-Anilino-3-Cyanoquinolines and Capecitabine A combination of a 4-anilino-3-cyanoquinoline compound (e.g. HKI-272, SKI-606, EKB-569) and a capecitabine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described.
CN101006831A Premixed compound fodder for fattening pig containing trace elements and vitamins The invention discloses a premixed fodder containing trace elements and vitamins for pigs, wherein the premixed fodder comprises the following constituents: ferrum 50-100mg/kg, zinc 80-160mg/kg, copper 100-200mg/kg, manganese 4-8mg/kg, vitamin A 15000-30000 international units, vitamin D3 2000-4000 international units, vitamin E 20-40 international units, vitamin K3 2-4mg, vitamin B1 2-4mg, vitamin B2 4-5mg, vitamin B6 2-4mg, vitamin B12 0.15-0.3mg, folic acid 1-2mg, nicotinic acid 5-10mg, calcium pantothenate 10-20mg, biotin 0.8-1.6mg. The invention can achieve high absorption ratio and improved pig production efficiency.
US20110002868 Cationic synthetic polymers with improved solubility and performance in surfactant-based systems and use in personal care and household applications The present invention is related to surfactant-based formulations comprising the polyelectrolytes and blends of such polyelectrolytes with non-cellulosic cationic polysaccharide polymers. The surfactant-based formulations exhibit improved clarity of the resulting formulations, their improved conditioning of keratin substrates, textile substrates, and hard-surface substrates, their improved deposition of dispersed phase materials onto keratin substrates, textile substrates, and hard-surface substrates, their improved lather performance, and their improved rheology in applications such as personal care and household care products and textile applications.
CN101313909A Corydalis saxicola total alkaloid extract injection powder injection and preparation method thereof The invention discloses Corydalis saxicola Bunting total alkaloid injection and a preparation method thereof (including water injection, powder injection and transfusion). The Corydalis saxicola Bunting total alkaloid injection is prepared by the given method through addition or no addition of auxiliary materials into Corydalis saxicola Bunting total alkaloids prepared by the given method. The product of the Corydalis saxicola Bunting total alkaloid injection has a better treatment effect, a simple preparation technique, and good market prospect and social benefit.
WO2008148215A1 Estrogen receptor-related receptor gamma (err gamma) in bone and cartilage formation and methods and compositions relating to same ERRγ is expressed in bone and cartilage in vivo and osteoblastic and chondrocytic cells in vitro. ERRγ is a transcriptional activator of an osteoblast-associated osteopontin (OPN) and chondrocyte-associated (Sox9) gene in osteoblasts and chondrocytes respectively. Knockdown of ERRγ expression by antisense oligonucleotide strategies in osteoblastic cell cultures reduces alkaline phosphatase activity. Together these findings indicate that ERRγ is expressed in and plays a functional role in bone and cartilage. The results also indicate that agonists and antagonists of ERRγ may be useful as therapeutic agents in a wide variety of diseases affecting bones and joints.
US20080139494 Introducing genetic material topically or by lavage into mucosal tissue cells of an individual, including rectal, vaginal, urethral, sublingual and buccal; used to deliver genetic material that encodes protein targets for immunization against pathogen infection, hyperproliferative or autoimmune diseases Methods of inducing mucosal immunity in individuals against proteins and peptides are disclosed. The methods comprise the step of administering topically or by lavage into mucosal tissue selected from the group consisting of rectal, vaginal, urethral, sublingual and buccal, a nucleic acid molecule that comprises a nucleotide sequence that encodes a protein or peptide that comprises an epitope against which mucosal immunity is desired. The methods may be used to immunize and individual against a pathogen infection, hyperproliferative diseases or autoimmune diseases using nucleic acid molecules which encode proteins and peptides that share an epitope with a pathogen antigen or protein associated with cells involved in hyperproliferative diseases or autoimmune diseases, respectively,
WO2011067348A3 Mek inhibitor salts and solvates thereof The present invention relates to sodium salt forms of 7-(4-Bromo-2-fluoro- phenylamino)-6-methyl-5-oxo-1,3,5-tetrahydro-indolizine-8-carboxylic acid (2- hydroxyethoxy)-amide and 7-(4-Bromo-2-fluoro-phenylamino)-5-oxo- 1,2,3,5-tetrahydro- indolizine-8-carboxylic acid cyclopropylmethoxy-amide and their corresponding solvates and polymorphs, which are useful in the treatment of a disease, disorder or syndrome associated with MEK inhibition, such as cancer, in mammals.
WO2007129473A1 Bicyclic aryl derivative The object is to provide a novel compound which has an S1P receptor agonist activity, can fully act as an immunosuppressant, has few adverse side-effects, and can be administered through the oral route. Disclosed is an S1P receptor agonist comprising a compound represented by the general formula (I), a salt thereof, or a solvate of the compound or the salt as an active ingredient. (I) wherein n represents 1, 2, 3 or 4; R1 represents a hydrogen atom or a C1-C6 alkyl group; R2 and R2a independently represent a hydrogen atom or a C1-C6 alkyl group, or R2 and R2a may together form a methylene group or an ethylene group; Ar1 represents a bivalent group derived from naphthalene, 1H-indole, 1H-pyrrolopyridine or benzofuran; and Ar2 represents a phenyl group which may have a substituent, a thienyl group which may have a substituent, an 1H-pyrazolyl group which may have a substituent or the like.
CN102846584A A veterinary preparation for treating gout in poultry The invention discloses a veterinary preparation for treating gout in poultry, comprising sodium citrate, potassium chloride and glucose. The invention can be used to effectively treat gout in poultry with remarkable curative effect and convenient application, and is worth popularizing.
CN102068451A Ointment for treating acne and preparation method thereof The invention relates to an ointment for treating acne and a preparation method thereof. The ointment is prepared from stearic acid, octadecanol, glycerin monostearate, glycerol, essence, distilled water, salicylic acid, erythrocin powder and borneol. When the ointment is used, the ointment is directly smeared on an affected part. After a medicament is absorbed through pores, a medicament directly kills bacterium on the affected part, circulates blocked pores and reduces the secretion of sebaceous gland so as to achieve a treatment effect. Clinical application proves that the curative ratio of the ointment is over 93 percent, and the ointment has no toxic or side effect.
WO2009046784A1 Pyridine derivatives useful as glucokinase activators Novel heterocyclic compounds of the formula (I) in which R1, R2, R3, R4 and D have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/o treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.
CN101513421A Application of 28-hydroxy-oleanane-2,11,13(18)-triene in preparing medicament for treating skin diseases The invention discloses application of 28-hydroxy-oleanane-2,11,13(18)-triene in preparing a medicament for treating skin diseases, and provides a pharmaceutical composition. The pharmaceutical composition is characterized by comprising the 28-hydroxy-oleanane-2,11,13(18)-triene (I) which is taken as an active component and one or more medicinal accessories. In the pharmaceutical composition provided by the invention, the medicinal accessories are all administrative accessories which are suitable for the skin or mucosa.
US7595156 Genes for synthesis of FR-008 polyketides The present invention relates to the base sequence of whole genes involved in the biosynthesis of FR-008 polyketides derived from Streptomyces sp. FR-008. This base sequence comprises genes coding for ketosynthase (KS), acyl transferase (AT), acyl carrier protein (ACP), ketoreductase (KR), dehydratase (DH) and enoyl reductase (ER) domains, and genes coding for modifier enzymes, such as ABC transporter, cytochrome P450 monooxygenase, ferredoxin, thioesterase, sugar synthetic protein, FAD-dependent monooxygenase, 4-amino-4-deoxychorismate (ADC) synthase and ADC lyase. The gene base sequence according to the present invention can be used to increase the productivity of the existing FR-008 polyketides or produce new FR-008 polyketides, through modification of its parts.
CN101185611A Technique for preparing silybin fine particles by using supercritical fluid crystallization technology The invention discloses a technique which applies a supercritical fluid crystallization technology to prepare minute grains of Silibinin. The technical steps comprise (1) preparation of Silibinin solution, one of ethanol or acetone is added into a solution pump and then the Silibinin solution is also added to the solution pump for preparing Silibinin solution; (2) feeding of carbon dioxide: CO2 is imported to a supercritical fluid antisolvent equipment system through a pressure regulating valve and then to a crystallization kettle; (3) the crystallization and precipitation of Silibinin: the Silibinin solution is quickly sprayed to the crystallization kettle through a nozzle and the minute grains of Silibinin are obtained at the bottom of the crystallization kettle; (4) inspection: the effective grain diameter of the obtained super minute grains is 10Mum+/-1Mum. The invention has the advantages that the technique of the invention is applicable for Silibinin crystal and is capable of preparing super minute grains which is beneficial for the absorption of human body, enhancing the dissolution rate and the medical effect of the Silibinin and reducing the using cost and the side effect of toxin. The Silibinin of the invention has special advantages in clinical treatment.
WO2014135524A1 Cabazitaxel and its use for treating metastatic prostate cancers The present invention relates to the compound having the following formula: (I), which may be in base form or in the form of a hydrate or a solvate, in combination with prednisone or prednisolone, for its use for the treatment of castration resistant or hormone-refractory metastatic prostate cancer in patients not at risk of developing gastrointestinal disorders chosen from the group consisting of: gastrointestinal bleeding and perforation, gastritis, enterocolitis, neutropenic enterocolitis, colitis, intestinal obstruction, and ileus.
WO2006012373A3 Combination therapies of hmgb and complement inhibitors against inflammation Compositions and methods are disclosed for treating a condition characterized by activation of an inflammatory cytokine cascade in a patient. The compositions comprise an HMGB A box and an inhibitor of complement biological activity, and/or an antibody that binds an HMGB polypeptide or biologically active fragment thereof and an inhibitor of complement biological activity, and/or an inhibitor of HMGB receptor binding and an inhibitor of complement biological activity. The methods comprise treating a cell or a patient with sufficient amounts of the composition to inhibit the release of proinflammatory cytokine(s) and/or inhibit the inflammatory cytokine cascade.
CN101690712B Sitafloxacin eye drop and preparation method thereof The invention discloses a sitafloxacin eye drop and a preparation method thereof. The sitafloxacin eye drop is prepared by mixing the following raw materials: 1-5mg of sitafloxacin, 0.1-5mg of antioxygen, 0.05-0.4mg of metal complexing agent, 1-40mg of a cosolvent, 1-20mg of an osmotic-pressure regulating agent, 0.13-5mg of a bacteriostatic agent and 0.1-1.3mg of surface active agent per litre offinished products. The invention can treat eye infectious diseases safely and effectively. The sitafloxacin eye drop prepared by the preparation method of the invention can obviously reduce impurities, increase stability, and improve product quality and curative effect.
US20100234316 Nucleoside Aryl Phosphoramidates for the Treatment of RNA-Dependent RNA Viral Infection The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.
US20100111988 Small peptide for anti-angiogenesis and use thereof The present invention relates to a small peptide for anti-angiogenesis and use thereof, in particular, to a small peptide useful for treating angiogenesis diseases; a polynucleotide coding the peptide; a vector and a cell comprising the polynucleotide; a pharmaceutical composition comprising the small peptide, the fused peptide or the fused protein, the polynucleotide, the vector and/or the cell. The small peptide, the fused peptide or the fused protein, the polynucleotide, the vector, the cell and/or the pharmaceutical composition can be used for treatment of associated diseases such as tumor by anti-angiogenesis.
US20120258058 Formulation with irritation reducing action comprising bisabolol and [6]-paradol The present invention relates to formulations having an irritation-reducing action, corresponding cosmetic and pharmaceutical products as well as associated methods and uses thereof.
EP1242009B1 Tissue sensitizing compounds for females with methods and apparatus for the delivery of these compounds The present invention comprises an apparatus such as a hand-manipulable, tissue stimulant-applying applicator (12, 14, 18) for use to apply a topical 'lip stimulating or a clitoral stimulating' compound (10) to the lips or the clitoral area of the human female.
WO2009128543A1 Process for producing silica-containing tablet, tablet, and composite particle for tablet Provided is a process for easily producing a tablet which contains silica produced at low cost. Also provided are: a silica-containing tablet produced by the process; and composite particles for producing the tablet. The process for producing a silica-containing tablet includes a step in which silica is kneaded together with a molten chemical or with an excipient other than silica and the resultant mixture is returned to ordinary temperature to thereby obtain composite particles for tablets.
CN101036643A Pharmaceutical composition containing arctigenin and preparation method A composition for medicine having arctigenin and a method for preparing the same. The composition includes arctigeni, oil, emulsifier and water which is capable of producing emulsion for oral taking and intravenous.
US7794739 composition for applying to skin containing at least one purine nucleic acid-related substance chosen from adenosine monophosphate and salt thereof, at least one pyrimidine nucleic acid-related substance chosen from uridine monophosphate and salt thereof, and at least one additive; anti-aging, anti-acne A method for effectively exerting a cell proliferation promoting effect of a purine nucleic acid-related substance, and a composition for cell proliferation containing a purine nucleic acid-related substance and a pyrimidine nucleic acid-related substance. Also a method for potentiating the cell proliferation promoting effect of the purine nucleic acid-related substance by using the purine nucleic acid-related substance in combination with the pyrimidine nucleic acid-related substance and a method for promoting cell proliferation, where the method includes the step of applying the purine nucleic acid-related substance in combination with the pyrimidine nucleic acid-related substance to the skin or mucosa.
EP2268647A2 Compounds and compositions for the detection and treatment of alzheimer's disease and related disorders One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyIoidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.
CN1771963A Medicine composition with enhanced antibacterial effect and its prepn The present invention discloses one kind of medicine composition. The medicine composition consists of cefalotin or its medicinal salt and sulbactam or its medicinal salt in the weight ratio of 0.5-4 to 0.5-4.
WO2009111948A1 The salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione or its derivatives, their polymorphs, preparation methods and uses thereof The present invention provides the pharmaceutically acceptable strong acid addition salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione, their solvates, preparation methods and uses of treating the diseases or abnormities of inhibiting inflammatory gene or new blood vessel formation . The water-solubility of the pharmaceutically acceptable strong acid addition salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione is higher than 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione. The present invention also provides the polymorphs of the pharmaceutically acceptable strong acid addition salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione and their solvates.
EP2325180A1 Chiral CIS-imidazolines There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V3, V2, R1, R2, R3, R4 and R5 are as herein described, processes for obtaining said compounds and pharmaceutical preparations containing them. These compounds are useful as anticancer agents, in particular as agents in the treatment of solid tumors.
EP1133285B1 A process for producing particles with a converted amorphous and/or meta-stable crystalline region into crystalline state The invention provides a process for crystallization of amorphous and/or meta-stable crystalline regions of preformed particles by treating the particles with a supercritical or subcritical fluid containing an anti-solvent and a solvent. The invention further provides formulations comprising particles produced according to the present process containing one or more pharmacologically active substances and one or more pharmaceutically acceptable excipients, use of said formulations in the treatment of an allergic and/or inflammatory condition of the nose or lungs and methods for treatment of such conditions.
CN101301298A Hyperlipemia prophylactic and therapeutic agent The objective of the invention is to provide a novel preventive therapeutic agent for hyperlipaemia. The inventive preventive therapeutic agent for hyperlipaemia is characterized by taking phenylethanoid glycosides compounds as effective ingredients. Moreover, the extracts include the phenylethanoid glycosides compounds as effective ingredients. The preventive therapeutic agent for hyperlipaemia preferably comprises at least one of echinacoside and acteoside as the phenylethanoid glycosides compounds, more preferably comprises both echinacoside and acteoside as the phenylethanoid glycosides compounds. In addition, the preventive therapeutic agent for hyperlipaemia is characterized by taking extracts of Orobanchaceae plants as effective ingredients. The extracts preferably comprises the phenylethanoid glycosides compounds as effective ingredients, and preferably comprises at least one of echinacoside and acteoside. The invention can be employed as medicaments for mammals including human beings, skin external agents, consumptive foods and feed for mammals.
WO2010125516A1 Compositions containing a mixture of lutein and zeaxanthine and coated with chocolate The present invention refers to pharmaceutical, dietary and/or nutraceutical compositions containing a mixture of lutein and zeaxanthin alongside at least one physiologically acceptable excipient. In particular the invention refers to orobuccal, sublingual and/or effervescent compositions formulated in form of tablet, capsule, granules or pill. The present invention also refers to the abovementioned compositions for use in the treatment, human or veterinarian, of diseases or disorders of the eye.
CN1861637A Preparation process of Huai Chinese yam polysaccharose and use thereof A process for extracting polyose from yam includes such steps as peeling, slicing, drying in the air, extracting in boiling water, filtering, centrifugal separation to obtain supernatant, adding alcohol, educing out, centrifugal separation of deposit to obtain crude polyose, dissolving in water, educing out, filtering and washing with absolute alcohol. It can be used for health-care food to decrease blood sugar, improve immunity, and delay senility.
EP1284722B1 Compositions containing a benzamide disulfide derivative for treating allergic diseases Methods and compositions for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The compositions contain a mast cell stabilizing disulfide derivative as an active ingredient.
WO2013021344A1 Imidazole derivatives as antiviral agents Compounds of the general formula (I) their tautomeric forms, their stereoisomers, their analogs, their prodrugs, their isotopes, their N-oxides, their metabolites, their pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as antiviral candidate, more specifically as anti-HCV are disclosed.
WO2014122646A1 Phosphorylcholine conjugates and uses thereof The present invention provides phosphorylcholine (PC)-conjugates and pharmaceutical compositions, particularly vaccines comprising same for the prevention or treatment of autoimmune diseases. In particular, the PC-conjugates of the present invention are effective in preventing or treating autoimmune diseases associated with pathological inflammation.
CN103565810A Compound preparation for preparing dextromethorphan or physiologically acceptable salts thereof and guaifenesin The invention belongs to the field of pharmaceutical preparations and relates to a compound syrup preparation composition for preparing dextromethorphan or physiologically acceptable salts thereof and guaifenesin. The compound syrup preparation composition consists of cane sugar, sodium benzoate, ethylparaben, citric acid, sodium citrate, pigments and essence. The compound preparation can be used for effectively relieving cough-related symptoms caused by respiratory tract infection and bronchitis, has a synergistic effect of medicines and also can be used for effectively and conveniently controlling the administration amount of a patient, and greatly reducing the children administration difficulty. Therefore, the dosage form has the characteristics that the compound preparation is high in dispersity, fast in absorption and fast in effectiveness after being taken by the patient, and the bioavailability of the medicine is improved.
WO2013017479A1 Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z4, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically- mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
WO2007052615A1 Pyridine derivative substituted by heterocycle and fungicide containing the same A fungicide which has excellent antifungal activity and is excellent in properties, safety, and metabolic stability. Also provided is a compound represented by the following formula (I) or a salt thereof: [Chemical formula 1] (I) [wherein R1 means hydrogen, halogeno, amino, C1-6 alkyl, C1-6 alkoxy, or (C1-6 alkoxy)C1-6 alkyl; R2 means hydrogen, C1-6 alkyl, amino, or di(C1-6 alkyl)amino; one of X and Y means nitrogen and the other means nitrogen or oxygen; ring A means a 5- or 6-membered heteroaryl ring or benzene ring each optionally having one or two halogen atoms or C1-6 alkyl groups; Z means a single bond, methylene, ethylene, oxygen, sulfur, -CH2O-, -OCH2-, -NH-, -CH2NH-, -NHCH2-, -CH2S-, or -SCH2-; R3 means hydrogen, halogeno, or C1-6 alkyl, C3-8 cycloalkyl, C6-10 aryl, 5- or 6-membered heteroaryl, or 5- or 6-membered nonaromatic heterocyclic group each optionally having one or two substituents selected from the substituent group (α); and R4 means hydrogen or halogeno].
WO2009133637A1 Sheet preparation for external use and sheet preparation set for external use It is intended to provide a sheet preparation for external use and a sheet preparation set for external use which efficiently and continuously generate hydrogen at lower cost. The sheet preparations for external use 6, 7 and a sheet preparation set for external use comprise a sheet 3 having an adhesive on one surface thereof and arranged thereon, a hydrogen storage porous material. The hydrogen storage porous material is preferably at least one member selected from the group consisting of hydrogen storage burned coral calcium, hydrogen storage zeolite, hydrogen storage charcoal, hydrogen storage activated carbon, hydrogen storage maifan stone, hydrogen storage tourmaline, and hydrogen storage rare earth mineral ore. The hydrogen storage porous material is preferably a tablet 1 provided with a concave portion 2 for receiving an organic acid 5. Further, the hydrogen storage porous material is preferably in a paste, powder, or granule form.
CN102150654A Additive composition for viscus function protection fluid The invention relates to an additive composition for viscus function protection fluid, which comprises 50 weight parts of anticoagulant and organic acid. A weight ratio of the anticoagulant to the organic acid is (15-35):(35-15). Preferably, the anticoagulant is natural hirudin or recombinant hirudin, and the organic acid is citric acid. When the composition is added into the protection fluid and the protection fluid protects isolated viscus, the protection fluid can achieve the anticoagulation effect, effectively prevent blood in the isolated viscus from clotting, and protect various functions of the isolated viscus; therefore, the composition can obviously improve the protection effect of the protection fluid on the isolated viscus.
US20110112085 Thiazolopyrimidine pi3k inhibitor compounds and methods of use Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
CN102961332A Liquid micellar preparation for increasing active closed-loop rate of camptothecin derivatives as well as preparation method and applications of preparation The invention belongs to the technical field of drugs, and in particular relates to a liquid micellar preparation for increasing the active closed-loop rate of camptothecin derivatives as well as a preparation method and applications of the preparation. The preparation disclosed by the invention is prepared from a amphiphilic copolymer, medicament molecules and an aqueous medium, wherein the amphiphilic copolymer is taken as a carrier material, the medicament molecules of active-dose camptothecin derivatives are physically loaded in a micellar form, and the aqueous medium is taken as a main dissolvent. The main body structure of the carrier material takes polyethylene glycol as a hydrophilic segment and takes polyester, poly-amino acid or polyether as a hydrophobic segment, and the medicament molecules are one or more of camptothecin, 10-hydroxycamptothecine, 9-nitrocamptothecin, 9-aminocamptothecin, 7-ethyl-10-hydroxycamptothecine, Topotecan, Irinotecan, Rubitecan, Exatecan, Belotecan, Karenitecin, Chimmitecan, Gimatecan, and the like. The micellar preparation can significantly improve the active closed-loop rate of the camptothecin medicament, enhances the medicament effect, and can effectively reduce the general reaction of the medicament, and therefore, the preparation is expected to be used in the cancer treatment of different stages.
WO2008125349A1 Spiro-pyrano-pyrazole derivatives The present invention relates to compounds of formula (I) having pharmacological activity towards the sigma (σ) receptor, and more particularly to some spiro-pyrano-pyrazole derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.
CN1830440A Metronidazule injection and its preparation method and use A liquid injection of metronidazole for treating anaerobe infection is prepared from metronidazole, sodium chloride, prepanediol, and the water for injection through dissolving the metronidazole in propanediol and conventional steps.
CN102432603A Preparation method and pharmacological effect of mangiferin hexa-butyl-esterified derivative The invention discloses a method for chemically synthesizing a mangiferin hexa-butyl-esterified derivative and a pharmacological effect of resisting inflammation and reducing blood sugar of the derivative. The chemical structural formula of the derivative is shown in the specifications. The derivative has a remarkable effect of inhibiting mouse auricle tumefaction caused by dimethylbenzene; and the derivative has a remarkable effect of treating diabetic mice induced by alloxan.
WO2013131406A1 Application of depolymerized sea cucumber glycosaminoglycans in preparing medicament for prevention and treatment of thromboembolic diseases Disclosed is an application of depolymerized sea cucumber glycosaminoglycans in preparing a medicament for prevention and treatment of thromboembolic diseases. The depolymerized sea cucumber glycosaminoglycans are more than one type of depolymerized sea cucumber glycosaminoglycans of weight-average molecular weights between 26,000 Da and 45,000 Da. During intravenous and subcutaneous injections, the medicament having the depolymerized sea cucumber glycosaminoglycans of weight-average molecular weights between 26,000 Da and 45,000 Da as active ingredients is provided with a significant anticoagulant effect, while at the same time, has minimal side effects, and is effective for use in the prevention and treatment of the thromboembolic diseases. For an injection of the depolymerized sea cucumber glycosaminoglycans of molecular weights between 26,000 Da and 45,000 Da, the blood coagulation time is extended while the anticoagulant effect is enhanced as the dosage increases, and medicament use is facilitated by subcutaneous administration when subcutaneous injection is employed for administration, while at the same time, convenience and safety of medicament use are improved.
CN103446130A Application of Lycojaponicumin B in liver cancer treatment drug The invention discloses application of Lycojaponicumin B in preparation of a liver cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Lycojaponicumin B also has remarkable inhabiting effect on growth of human liver cancer cell strains HepG2, MHCC-LM3, Be1-7402 and HuH-7. Therefore, the Lycojaponicumin B can be used for preparation of an anti-liver cancer drug and has good development and application prospect. The application of the Lycojaponicumin B in the preparation of the liver cancer treatment drug is disclosed for the first time. Due to the fact that the fact that the skeleton type is a novel skeleton type, and the high liver cancer cell inhibiting activity of the Lycojaponicumin B is previously unimagined.
CA2559700C Benzoxazine for treating respiratory tract diseases The invention relates to the use of compounds of general formula (1), wherein the radicals R1, R2 and R3 can have the meaning cited in the claims and in the description. The invention also relates to the production of a medicament for treating respiratory tract diseases.
WO2008008981A1 Interleukin 21 and tyrosine kinase inhibitor combination therapy The present invention provides methods for use of IL-21 in combination with a tyrosine kinase inhibitor (TKI) in treatment of diseases in which inhibition of phosphorylation via TK inhibition and modulation of immune function play a clinically beneficial role. These diseases include, but are not limited to, cancers, such as renal cell carcinoma and metastatic melanoma.
CN101805336A Compound containing tryptophane and isoxazole skeleton and preparation method and application thereof The invention relates to the medicine filed related to diabetes, in particular to a peroxisome proliferator-activated receptor (PPAR) agonist which has the general formula I shown in the specification, has treatment effect on diabetes and contains tryptophane and an isoxazole skeleton, a preparation method of the PPAR agonist and application of the PPAR agonist in preparing medicines for treating diabetes, wherein, the group definition refers to the specification.
US20120244212 Enhanced method and composition for the treatment of hiv+ tuberculosis patients with anti-retroviral drugs and liposomal encapsulation for delivery of reduced glutathione The invention is the use of a therapeutically effective amount of glutathione (reduced) in a liposome encapsulation for oral administration to improve symptoms of illnesses that are related to tuberculosis and HIV and more generally viruses and for the treatment and prevention of virus, particularly HHV-6 and EBV, which liposomal encapsulation of glutathione (reduced) is referred to as liposomal glutathione. The application references specifically reduced glutathione and its importance, and how to stabilize it effectively so it can be taken orally, and need not be refrigerated. New uses for tuberculosis are discussed. The combination is proposed of reduced glutathione and Highly Active Anti-Retroviral Therapy having at least one pharmaceutical composition selected from the group of Nucleoside/tide Reverse Transcriptase Inhibitors (NRTIs), Protease Inhibitors (PIs), and Non-nucleoside Reverse Transcriptase Inhibitors (NnRTIs), and further anti-tuberculosis drugs.
WO2014152537A1 P2x7 modulators The present invention is directed to a compound of Formula (I) Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I) and methods comprising administering to a subject at least one compound selected from compounds of Formula (I) for treating diseases mediated by P2X7 receptor activity, such as rheumatoid arthritis, osteoarthritis, psoriasis, septic shock, allergic dermatitis, asthma, allergic asthma, mild to severe asthma, steroid resistant asthma, idiopathic pulmonary fibrosis, allergic rhinitis, chronic obstructive pulmonary disease; airway hyper-responsiveness, diseases of the nervous and neuro-immune system, acute and chronic pain states of neuropathic pain, inflammatory pain, spontaneous pain, opioid induced pain, diabetic neuropathy, postherpetic neuralgia, low back pain, chemotherapy-induced neuropathic pain, fibromyalgia, diseases involved with and without neuroinflammation of the central nervous system, mood disorders, major depression, major depressive disorder, treatment resistant depression, bipolar disorder, anxious depression, anxiety, cognition, sleep disorders, multiple sclerosis, epileptic seizures, Parkinson's disease, schizophrenia, Alzheimer's disease, Huntington's disease, autism, spinal cord injury and cerebral ischemia/traumatic brain injury, stress-related disorders, diseases of the cardiovascular, metabolic, gastrointestinal and urogenital systems such as diabetes, diabetes mellitus, thrombosis, irritable bowel syndrome, irritable bowel disease, Crohn's disease, ischemic heart disease, ischaemia, hypertension, cardiovascular disease, myocardial infarction, and lower urinary tract dysfunction such as incontinence, lower urinary tract syndrome, Polycystic Kidney Disease, Glomerulonephritis, skeletal disorders, osteoporosis, osteopetrosis, and glaucoma, interstitial cystitis, cough, ureteric obstruction, sepsis, Amyotrophic Lateral Sclerosis, Chaga's Disease, chlamydia, neuroblastoma, Tuberculosis, and migraine.
US20090030089 Silicon Substituted Oxyapatite The invention is a silicon substituted oxyapatite compound (Si—OAp) for use as a synthetic bone biomaterial either used alone or in biomaterial compositions. The silicon substituted oxyapatite compound has the formula Ca5(PO4)3-x(SiO4)xO(1-x)/2, where 0. An independent claim is included for a method for the preparation of (A). - ACTIVITY : Ophthalmological. No biological data given. - MECHANISM OF ACTION : None given.
EP0871448B1 Aryl and heteroaryl quinazoline compounds which inhibit csf-1r receptor tyrosine kinase This invention relates to the modulation and/or inhibition of cell signaling, cell proliferation, cell inflammatory response, the control of abnormal cell growth and cell reproduction. More specifically, this invention relates to the use of mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in inhibiting cell proliferation, including compounds which are useful protein tyrosine kinase (PTK) inhibitors. The method of treating cell proliferation and/or differentiation or mediator release using said quinazoline compounds and their use in pharmaceutical compositions is described.
WO2007027569A1 Activated carbon and use thereof for reducing or maintaining body weight The present invention is generally directed towards compositions including activated carbon and methods of use thereof such as for reducing or maintaining body weight in a subject. In one embodiment, a dietary supplement comprising a composition including amorphous activated porous carbon particles, with a total surface area not less than about 700 m2 per g and interstitial mesopores having a mean radius of not less than about 2 nm and not greater than about 50 nm, is administered to a subject in an amount sufficient, which may include from about 50 mg to about 50 g of activated carbon per dose, and for a duration sufficient, to reduce dietary uptake in the subject to reduce or maintain the body weight of the subject.
WO2008025361A1 3-(1h-indol-3-yl) indan-1-ylamine derivatives for the treatment of depression and anxiety The invention provides novel indane compounds which are useful in the treatment of affective disorders, pain disorders, attention deficit hyperactivity disorder (ADHD), cognitive disorders, substance abuse, smoking cessation and stress urinary incontinence. The compounds are inhibitors of serotonin, norepinephrine and dopamine re-uptake.
CA2219659C Rapamycin derivatives Compounds of Formula (I), wherein R2 is selected from formula (II) or formula (III), and X is OH or H show immunosuppressant activity.
CN101288741A Medicinal composition for preventing birth defect and improving memory and intelligence The invention relates to a medicine combination which is used for preventing birth defects and improving memory and intelligence. The combination comprises atractylodes, rhizoma polygonatum, compound vitamin B and trace elements including zinc and selenium, which is essentially applied to women before pregnancy, pregnant women and lactating women; the combination is effective in preventing the birth defects and improving memory and intelligence and is provided with the function of health invigoration and can not produce any side effects even being used for a long time.
EP1689718A1 1-amino-isoquinoline derivatives for the treatment of diseases associated with inappropriate alk5 activity A compound of Formula (I) wherein R1 represents a phenyl or napthyl group (each of which is optionally substituted by one or more substituents independently selected from -OH, -C1-6alkyl, C1-6haloalkyl, -OCH2OCH3, -C1-6alkoxy, -halogen,), or a mono or bicyclic heteroaryl group comprising 1, 2 or 3 nitrogen atoms, optionally substituted by -C1-6alkoxy, -C1-6alkyl, C1-6haloalkyl or =0; R2 represents H, benzoimidazolyl, benzothiazolyl, isoquinolinyl, or quinolinyl group or phenyl (said phenyl being optionally substituted by -NR3R4, -C1-4alkoxy, -C1-6alkyl, -CONR3R4, -SO2NR3R4, -NHCONR3R4, -NHCOC1-6alkyl, -C1-6haloalkyl, -OCH2O-, -phenoxy (wherein the phenyl moiety is optionally substituted by NH2 ), -C1-3alkyl, -C1-3alkoxy, -CF3, -5 membered heteroaryl group comprising one or two nitrogen atoms). R3 and R4 are independently selected from H, -C1-6alkyl, -C1-3alkylNR5R6; R5 and R6 are independently H or C1-3alkyl; or a salt, solvate, or physiologically functional derivative thereof.
CN1640405A Method for producing d-alpha-succinic tocopherol granule The present invention relates to a production method of d-alpha-succinic acid tocophenol granules. Said method includes the following steps: a. adding d-alpha-succinic acid tocophenol raw material and adhesive into a stirring type granulating machine, mixing them for 1-10 min, and the described adhesive is ethl cellulose solution; b. cutting the mixture obtained by step a in stirring type granulating machine for 1-10 min.; and c. drying the granules obtained by step b. and sieving.
US7351732 Serotonin (5-hydroxytriptamine, 5-HT) 5-HT1A receptor subtype agonists; neuroprotective agents; cerebral damage due to traumatic or ischemic stroke; 2-[4-[(Chroman-2-yl)methylamine]butyl]-1,3-dioxoperhydropyrrolo[1,2-c]imidazol New cycloalkanedione derivatives that are serotonin (5-hydroxytriptamine, 5-HT) 5-HT1A receptor subtype agonists and, consequently, they are useful in the treatment of pathological states for which an agonist of these receptors is indicated. They are particularly useful as neuroprotective agents, of special interest in the treatment and prophylaxis of cerebral damage produced by traumatic or ischemic stroke. In general terms, said cycloalkanedione derivatives correspond to formula I:
CN103655599A Polysaccharide composition, application and medicinal preparation containing same The invention provides a polysaccharide composition, application and a medicinal preparation containing the same. The polysaccharide composition comprises the following substances in parts by weight: 20-90 parts of mulberry leaf polysaccharide, 20-90 parts of balsam pear polysaccharide, 10-80 parts of polygonatum rhizome polysaccharide and 10-40 parts of matrimony vine polysaccharide. The product has blood sugar reducing effect, is capable of maintaining islet cells, is helpful for enhancing human body immunity, and especially is helpful for enhancing the self resistant and regulating capabilities of weak diabetes patients; and the various polysaccharide compositions have the synergic effect, so that a diabetes pathological position is affected by multiple targets, and the product has obvious blood sugar reducing effect.
US20100047330 Treatment for dark adaptation The present invention addresses the treatment of age-related macular degeneration using regulation of pathogenic mechanisms similar to atherosclerosis. In further specific embodiments, compositions that increase reverse cholesterol transport are utilized as therapeutic targets for age-related macular degeneration. In a specific embodiment, the lipid content of the retinal pigment epithelium, and/or Bruch's membrane is reduced by delivering Apolipoprotein A1, particularly a mimetic peptide.
EP2344144A1 1-amino-alkylcyclohexane derivatives for the treatment of cognitive impairment in tinnitus The present invention relates to the treatment of an individual afflicted with cognitive impairment associated with tinnitus comprising administering to the individual an effective amount of a 1-amino-alkylcyclohexane derivative.
EP2779839A1 Products for oral administration comprising extracts of punica granatum (pomegranate), intended for a pet, and applications of same The invention relates to a product for oral administration intended for a pet, comprising extracts of punica granatum (pomegranate). The invention is characterised in that the invention further comprises at least two additional antioxidant compounds chosen from: - soya isoflavone extracts; - L-carnitine; and - taurine.
US20120220591 Pyrimidone compounds A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents hydrogen atom and Y represents hydroxyl group, or X represents fluorine atom and Y represents hydrogen atom; R1 represents a C1-6 alkyl group; R2 represents a morpholin-4-yl group which may be substituted, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
US6849640 Such as 8-(2,4-dichlorophenyl)-2,3,4,4a,5,9b-hexahydro-1H-pyrido(4,3-b)indole for use as HT3 receptor antagonist, for treatment of depression and obesity The present invention provides 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating diseases wherein modulation of 5-HT activity is desired.
US7651681 Method and compositions for in situ formation of protective and/or medicated films on body tissue Methods and compositions for forming protective and/or medicated films on body tissue. Liquid compositions contain a hydrophobically modified polymer, other than an esterified lower-hydroxyalkyl-substituted cellulose, suspended or dissolved in a solvent. The modified polymer is soluble in the solvent but insoluble in body fluids. The compositions may optionally contain a separate medicinal component, i.e., one which is present in addition to any medications, if any, present in the solvent, in the modified polymer and in any other additive components such as flavors, skin penetrants, preservatives, other solvents for the additives, etc. A protective and/or medicated film is formed in situ upon body tissue by applying the liquid composition to the tissue and separating the solvent from the composition, e.g., by vaporization.
US20090234023 Substituted hydroxyacetophenone derivatives The present invention relates to substituted hydroxyacetophenone derivatives having antiproliferative and antimicrobial properties, to pharmaceutical compositions containing them, as well as to a method of preparing them. Moreover, the hydroxyacetophenone derivatives according to the invention can serve as organic intermediates for the preparation of biologically active compounds.
CN101838263A Benzimidazole derivative with cardiovascular activity and preparing method and application thereof The invention discloses benzimidazole derivative, belonging to the field of the medicinal chemistry. The invention also discloses a preparation method of the benzimidazole derivative, the medicinal composition containing the compound of benzimidazole derivative and the application of the compound of benzimidazole derivative to the treatment of hypertension and congestive heart failure and the treatment of other diseases through doubly blocking angiotensin II (AT1) receptor and endothelin (ETA) receptors.
US20080311040 METHODS AND COMPOSITIONS FOR IMPROVED THERAPEUTIC EFFECTS WITH siRNA The present invention relates to chemically modified, linked double-stranded (ds)RNA compositions comprising two or more double-stranded (ds) oligoribonucleotides linked by at least one linking moiety and methods of formulating and delivering such compositions to modulate gene expression through target-specific RNA co-interference (RNAco-i). The compositions of the invention may optionally comprise a conjugation or a complex with one or more small molecule drugs, protein therapeutics, or other dsRNA molecules. The present invention is directed at the methods of production for, methods of use of, and therapeutic utilities for RNAi co-interference therapy utilizing the compositions of the invention.
WO2014046129A1 Pharmaceutical composition for oral administration with improved elution and/or absorbency This pharmaceutical composition for oral administration contains, as an active component, a 4-((1-methylpyrrole-2-yl)-carbonyl)-N-(4-(4-morpholine-1-yl-carbonyl piperidine-1-yl)-phenyl)-1-piperazinecarboxamide or a salt or solvate thereof, and contains, as an acidic additive, adipic acid, succinic acid, fumaric acid, L-aspartic acid, L-glutamic acid, or any combination of these.
US20120178806 Pharmaceutical formulations comprising 9-cis-retinyl esters in a lipid vehicle Pharmaceutical formulations comprising 9-cis-retinyl esters in a lipid vehicle are described as retinoid replacement therapies for treating retinal degenerations in humans.
WO2009020561A3 Compositions and methods of use thereof, for the treatment of oral pain, comprising cloves or extract thereof in combination with a steroid Provided are compositions for delivery to an individual's mouth to provide immediate as well as long-lasting pain relief, particularly after tooth extraction or other dental procedure, which include clove, a clove extract or eugenol, and optionally a steroid and other additives including an antibiotic. Kits and systems for delivery of the composition to provide sustained pain relief are also provided.
US7285568 Substituted p-(2-alkoxy-2-acylethyl)biphenyl compounds, e.g., 1-[4'-(2-ethoxy-3-morpholin-4-yl-3-oxopropyl)biphenyl-3-yl]-3-heptyl-1-methylurea; useful in human or veterinary medicine: dermatology, cardiovascular diseases, immune diseases, and diseases associated with lipid metabolism Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
US20070015800 Use of a compound in providing refreshedness on waking and a method for the treatment of drowsiness therewith There is disclosed the use of triprolidine for enabling an individual to wake refreshed after sleep and the method of treating such an individual with triprolidine. The triprolidine is administered shortly before a person wishes to fall asleep, preferably orally and most commonly in the form of a tablet containing less than 5 mg, eg 0.1 mg, 1.25 mg or 2.5 mg, of the active ingredient. The triprolidine is also effective in enabling an individual to sleep more easily.
EP2571577A1 Improved immunotherapeutic dosing regimens and combinations thereof The invention described herein relates to therapeutic dosing regimens and combinations thereof for use in enhancing the therapeutic efficacy of immunotherapeutic agents e.g. CTLA-4 antagonists such as 3pilimumab or Tremelimumab in combination with one or more chemotherapeutic agents in cancer patients.
CN103443099A Compositions and methods for modulating FXR The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).
US20100144762 Novel sulfonamides as l-cpt1 inhibitors The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
WO2010058402A1 Novel anti-biofilm agents Novel agents exhibiting anti-biofilm formation activity while being non-cytotoxic are provided, as well as methods of using the same, either per se or conjugated to a polymer, for preventing and/or reducing the formation of microbial biofilms and/or for disrupting microbial biofilms. The novel agents described herein include thiazolidine-2,4-diones (TZDs), pyrrolidine -2, 5- diones (PYDs), imidazolidine-2, 4 -diones or oxazolidine-2,4-diones, substituted by an alkylidene having 7-20 carbon atoms in its backbone chain.
CN101278921A Triopisetron Hydrochloride microcapsule and method for preparing injection The invention provides a tropisetron hydrochloride freeze-dry preparation for treating emesis, containing tropisetron hydrochloride, gelatin, dextran, oleophilic emulsifier, hydrophilic emulsifier and freeze-dry supporting agent. The invention also relates to a preparation method of the tropisetron hydrochloride freeze-dry preparation, containing the following steps: (1) the tropisetron hydrochloride is added into injection water and completely dissolved; (2) the gelatin and the oleophilic emulsifier are added in solution prepared in step (1) to prepare water-in-oil emulsion; (3) dextran solution and the hydrophilic emulsifier are added in the solution prepared in step (2) to prepare water-in-oil-in-water double emulsion; (4) the prepared double emulsion is dropped by bolus injection into strong base solidified liquor in a high-voltage electrostatic field by an orifice; after solidifying, a microcapsule is filtered and washed by water or PH regulator to lead PH to be 5-7; (5) the freeze-dry supporting agent is dissolved in the injection water and mixed with the microcapsule evenly; after subpackage and freeze drying, the tropisetron hydrochloride freeze-dry preparation is obtained.
WO2012101605A1 Fgf receptor-activating 3-o-alkyl oligosaccharides, preparation thereof and therapeutic use thereof The invention relates to the FGF receptor-activating oligosaccharides corresponding to formula (I) in which R1 represents an optionally substituted -O-alkyl group, R2 represents a hydroxyl group or an -O-alkyl group, R3, R5, R6, R7 and R8 represent -OSO3- or hydroxyl groups, R4 represents an NH-CO-alkyl or -O-alkyl group, R represents an -O-alkyl group, and n and m, which may be identical to or different from one another, represent integers equal to 0 or 1. Method for the preparation thereof and therapeutic use thereof.
CN1903204A Methionine vitamin B1 for injection and its prepn. method A freeze-dried powder injection of methylthio-aminoacids VB1 contains methylthio- aminoacids, VB1 and excipient. Its preparing process is also disclosed.
WO2014148455A1 Terpenoid derivative Provided is a novel terpenoid derivative which exhibits anti-inflammatory action and cytoprotective action by activating Keap1/Nrf2/ARE signal transduction pathways. Terpenoid derivative A is represented by formula (1).
WO2007008942A3 Phenylamino-acetic acid [1-(pyridin-4-yl)-methylidene]-hydrazide derivatives and related compounds as modulators of g protein-coupled receptor kinases for the treatment of eye diseases Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer osteoporosis and glaucoma are also provided. (Formula (I)). A is selected from a heteroaryl group (i): wherein X1, X2, X3 and X4 are, independently, CH, O, S or N-R6, with the proviso that at least one of X2 or X3 is O, S or N-R6; and a heteroaryl group (ii): wherein X5 and X9 are CH or C-halogen, X6 and X8 are CH, and X7 is N, and wherein the six-membered heteroaryl group may be further fused with an unsubstituted six-member aryl group; R1, R2, R3, R4, and R5 are, independently, hydrogen; halogen; C1-C4 alkyl; amino; nitro; cyano; heteroaryl; carboxy, carbonylamino; aminosulfonyl; sulfonylamino; aminoacyl; thioalkyl; sulfonyl; acyl; heterocycle; -OR; -O-C1-C4alkyl-heterocycle; -C(O)NH-C1-C4alkyl-heterocycle; -C(O)NH-heteroaryl; -C(O)NH-aryl; or carboxylamino; wherein R is C1-C4 alkyl; aryl, heteroaryl, C1-C4 alkyl aryl or C1-C4 alkyl heteroaryl; R6 is H or C1-C4 alkyl; R7 is hydrogen, C1-C4 alkyl or C1-C4 alkoxy; and X is N-R6.
CN101486686B Two compounds with quinoxaline mother ring and preparation thereof The invention relates to a new compound and a preparation field thereof and provides two compounds containing a quinoxaline mother rotor: 3-methyl-2-ethoxycarbonyl-quinoxaline-1, 4-dioxide (a compound I) and 2-acetyl-3-phenyl-quinoxaline-1, 4-dioxide (a compound II) and a preparation method thereof. The existing quinoxaline medicaments are widely applied to the antisepsis and growth promotion of animals, but such problems as medicament residual, reproductive toxicity and other aspects appear if the medicaments are applied in a long run. The two quinoxaline compounds have the advantages of strong resistance to bacteria and low toxicity. The two compounds with the quinoxaline mother rotor can be applied to the growth promotion of animals, and the preparation of antimicrobial agents, feedstuff or additives.
US20090197878 SUBSTITUTED BENZO[d][1,3]OXAZIN-2(4H)-ONES AND RELATED DERIVATIVES AND THEIR USES FOR MODULATING THE PROGESTERONE RECEPTOR Compounds of formula (I), or pharmaceutically acceptable salts thereof, are provided, wherein R1-R6 and X are defined herein. Also provided are methods of preparing the compounds of formula (I), pharmaceutical compositions and kits containing a compound of formula (I), as are methods of treating endometriosis, hormone-dependent carcinomas, leiomyoma, fibroids, dysfunctional bleeding, polycystic ovary syndrome, and menopause related symptoms; methods of contraception; methods of providing hormone replacement therapy; methods of stimulating food intake; methods of synchronizing estrus; and methods of treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder by administering to a mammal in need thereof a pharmaceutically effective amount of a compound of formula (I).
CN102138889A Targeted drug-bearing ultrasonic microbubble and preparation method thereof The invention relates to a targeted drug-bearing ultrasonic microbubble comprising a lipide dimolecular layer outer shell, targeted polypeptide fixed at the outer side of the lipide dimolecular layer outer shell, a biological inert gas wrapped in the lipide dimolecular layer outer shell and medicament granules dispersed in the lipide dimolecular layer outer shell. The targeted polypeptide is a polypeptide or protein derivative containing an amino acid sequence CGNKRTRGC. By connecting the polypeptide or protein derivative containing a tumor targeted peptide sequence outside the lipide dimolecular layer outer shell, the obtained targeted drug-bearing ultrasonic microbubble can target the lymph vessels and the tumor cells of a tumor, can detect and diagnose the generation, the development and the curative effect on the tumor in real time through high-frequency ultrasonic imaging and can crush the microbubble through low-frequency ultrasound to release the medicament granules so as to achieve the aim of controllably and targetedly releasing the medicament, thereby having extremely important meanings to the prevention, diagnose and treatment of the tumor. In addition, the invention also relates to a preparation method of the targeted drug-bearing ultrasonic microbubble.
US7220745 Viricides; therapy for hepatitis virus infections The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.
WO2014071832A1 Alk kinase inhibitors Disclosed herein are ALK kinase inhibitors, pharmaceutical compositions thereof, and pharmaceutical uses thereof. More particularly disclosed herein are compounds of Formula (I), wherein each substituent of Formula (I) is defined as in the description.
CN101108162A Pharmaceutical composition treating ringworm of the nails, extremity tinea and method of manufacturing the same The invention discloses a medicine combination for curing onychomycosis and tinea manuum and pedis, which comprises an ointment and a liquid medicine that are prepared and applied independently. Wherein, the ointment comprises the following components with relevant weight shares: Vaseline of 50-70 shares, urea of 30-50 shares and resorcinol of 25-30 shares; the liquid medicine comprises the following components with relevant weight shares: distilled water of 80 to 120 shares and glacial acetic acid of 20 to 40 shares. The ointment in the invention has outstanding effects of eliminating true fungus and softening the affected nail; the liquid medicine has the effects of sterilizing and preventing the relapse, ensuring strong penetration and realizing double effects for curing and promoting the growth of new nail. With the coordination of the two medicines, the fungus can be eliminated and the affected disease source area can be completely sterilized, thus thoroughly curing the onychomycosis, realizing outstanding treatment effect for tinea manuum and pedis. Besides, in clinical medication, the invention results in no adverse reaction and ensures reliable treatment effect.
WO2014064166A1 Mixed inhibitors of aminopeptidase n and of neprilysine Mixed inhibitors of aminopeptidase N and of neprilysine are described. Pharmaceutical compositions containing at least one of these compounds, used alone or in combination with morphine and derivatives thereof, endocannabinoids and inhibitors of the metabolism thereof, GABA derivatives such as gabapentin or pregabalin, duloxetine or methadone, can be used as an analgesic, anxiolytic, antidepressant or anti-inflammatory.
CN1623548A Galanthamine slow release preparation and its preparation method A slow-releasing jilkon is prepared from jilkon and conventional slow-releasing additive. Its advantages are high durability and low by-effect.
CN101849933B Conjugated linoleic acid ferrite preparation and preparation method thereof The invention discloses a conjugated linoleic acid ferrite preparation and a preparation method thereof. The conjugated linoleic acid ferrite preparation is prepared by the following raw materials by molar ratio: conjugated linoleic acid: soluble ferrite = 2:1.05-1.60. The preparation method comprises the following steps: at room temperature or near room temperature, conducting saponifiacation reaction between conjugated linoleic acid with biological functional activity and alkali metal hydroxides or alkali alcoholate at first, and then conducting reaction with soluble ferrite solution to obtain the conjugated linoleic acid ferrite. The synthesized conjugated linoleic acid ferrite can be used in functional additives of nutriments, medicinal components and feed additives. The method of theinvention has the advantages of even reaction, simple technology, easy operation, high ferrite preparation purity and stable quality, and is particularly suitable for application fields with high requirements on products.
US7666876 Buprenorphine formulations for intranasal delivery Aqueous formulations suitable for intranasal administration comprise buprenorphine or a physiologically acceptable salt or ester thereof and (a) a pectin having a degree of esterification of less than 50%, (b) chitosan and a polyoxyethylene-polyoxypropylene copolymer (poloxamer) or (c) chitosan and hydroxypropylmethylcellulose. Such formulations can induce rapid and prolonged analgesia when delivered intranasally to a patient. The buprenorphine or buprenorphine salt or ester may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration of buprenorphine, Cther, of 0.2 ng/ml or greater which is maintained for a duration Tmaint of at least 2 hours.
US20050059688 administering nontoxic, preferential and potent c-kit ligand inhibitors such as imatinib, to humans for treatment of inflammatory diseases such as rheumatoid arthritis The present invention relates to a method for treating inflammatory diseases such as rheumatoid arthritis (RA), comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.
US20100015225 Solid dispersion of a neurokinin antagonist Solid dispersion comprising (4R)-4-[N′-methyl-N′-(3,5-bistrifluoromethyl-benzoyl)-amino]-4-(3,4-dichlorobenzyl)-but-2-enoic acid N—[(R)-epsilon-caprolactam-3-yl]-amide or a pharmaceutically acceptable salt or solvate thereof and a carrier. Pharmaceutical compositions comprising such solid dispersion are useful to treat patients who have functional motility disorders of the viscera, especially irritable bowel syndrome or functional dyspepsia, or urinary bladder disorders, especially urinary incontinence.
CN103316009A Application of Aspeverin in preparation of medicine for treating cervical carcinoma The invention discloses an application of Aspeverin in the preparation of a medicine for treating cervical carcinoma and belongs to the technical field of new application of medicines. It is found through in vitro MTT antineoplastic activity rating that Aspeverin also has a remarkable effect of inhibiting the growth of human cervical carcinoma cell strains HELA, HELA 229, HCE1 and CASKI. Thus, Aspeverin can be used in the preparation of an anti-cervical carcinoma medicine and has a good development and application prospect. The application of Aspeverin in the preparation of a medicine for treating cervical carcinoma is disclosed for the first time. In addition, Aspeverin has an unexpectedly strong inhibitory activity of cervical cancer cell.
WO2009038671A2 Oxylipin compounds for treating autoimmune diseases The invention relates to methods of modulating immune function, suppressing immune response, treating autoimmune diseases or autoimmune disorders, and treating diseases, sequelae or pathological conditions mediated by an activation of the imune system comprising administering a compound of formula A, a compound of any one of formulae 1 -49, a lipoxin compound, or an oxylipin compound.
EP1948182A1 Method for treating neuronal and non-neuronal pain A method for the combined treatment of neuronal and non-neuronal pain in mammals is provided comprising administration of adenylyl cyclase 1 inhibitors having the following general formula (1): (1) wherein: G, H, J and M are each N, or H and J are each C, and G and M are each N, S or O, or H, J and M are each C and G is N, S or O.
US20100209401 Use of SDF-1 to Improve Ischemic Myocardial Function A method is provided for increasing trafficking of endothelial progenitor cells to an ischemic myocardium in a subject's heart comprising administering to the subject's heart an amount of Stromal-Derived Factor-1 (SDF-1).
CN101230059A Bicycle aza alkyl derivative, preparation method and use in medicine thereof The invention relates to a novel dicyclic aza alkane derivative shown in a general formula (I), the preparation method thereof, a medicine composition containing the derivative and the use thereof as a therapeutical agent, especially a dipeptidyl peptidase inhibitor (DPPIV), wherein, each substituent of the general formula (I) is as defined in the instruction.
WO2007099302A3 Methods of maintaining oral health in animals using morpholine derivatives Use of a compound having the formula (I) in the manufacture of a medicament for the prevention or treatment of a disease caused by oral bacteria in an animal wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholiπo ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, or a pharmaceutically acceptable salt thereof. A cosmetic method of preventing or decreasing oral staining in an animal, comprising the step of exposing the oral cavity to a morpholino compound of general
WO2013182862A1 Synergistic therapies of cannabidiol with hypothermia for neuroprotection The present invention relates to the combination of the phytocannabinoid cannabidiol with therapeutic hypothermia for use in the treatment of neuroprotection or astroprotection.
CN102552923A Pharmaceutical composition containing L-carnitine and coenzyme Q10 as well as its preparation method The present invention provides a pharmaceutical composition containing L-carnitine and coenzyme Q10 as well as its preparation method. The pharmaceutical composition comprises L-carnitine or its pharmaceutically acceptable salt or ester, coenzyme Q10 or its pharmaceutically acceptable salt or ester, and a solubilizing agent, wherein the solubilizing agent comprises one or more selected from polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, stearic acid polyoxyethylene ester and polyethylene glycol 15 hydroxy stearate . The prepared pharmaceutical composition which takes L-carnitine and coenzyme Q10 and/or their pharmaceutically acceptable salts as an active ingredient has the advantages of good stability, high security, stable preservation for long-term and safe usage; and the pharmaceutical composition can fully perform the synergy of two ingredients, has the merits of convenient usage, economical and practical effects, and possesses a good prospect.
CN102949399A Application of tanshinone IIA in preparation of medicines inhibiting keratinocyte proliferation diseases The invention relates to an application of tanshinone IIA in the preparation of medicines inhibiting keratinocyte proliferation diseases. The keratinocyte proliferation diseases comprise psoriasis, ichthyosis and keratinocyte tumors. According to the invention, a new use of the tanshinone IIA in the pharmacy is excavated, so a new application field is developed; the tanshinone IIA has a good treatment effect on skin diseases caused or characterized by the keratinocyte over-proliferation, such as the psoriasis, the ichthyosis and the keratinocyte tumors; the tanshinone IIA has been clinically used in other medicines, and a case that the tanshinone IIA has extremely small toxic side effects is proved, so the tanshinone IIA can be safely used; and the tanshinone IIA has the advantages of abundant raw material source, low price, simple preparation technology, wide industrialization prospect, and suitableness for the wide popularization and use.
WO2006136829A3 Pyrazole derivatives and their use as pka and pkb modulators The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof; wherein A is a saturated hydrocarbon linker group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; L1 is a bond or a linker selected from C1-C4 alkenylene, C1-C4 alkynylene, -CONR’, -NR’CO, -S-, -C(O)-, -C(NR11)-, -C(S)-, -N(R11)2, C(=CHR11), -SO- and -SO2-; or L1 together with t R16 forms an 8-12 membered fused bicyclic heteroaryl ring system; L3 is a bond or a linker selected from CONH and HNCO; provided that L1 and L3 cannot both be linkers simultaneously; and provided also that L1 and L3 cannot both be a bond simultaneously; R16 is an optionally substituted 5- to 12-membered monocyclic or bicyclic carbocyclic or heterocyclic ring; L2 is absent or is a linker selected from C]-C4 alkylene, Ci-C4 alkenylene, Ci-C4 alkynylene, -CONR’-, -NR’CO-, -O-, -S-, -C(O)-, C(=CHR11), C(S)-, -N(R11)2, C3-4 cycloalkanediyl, -SO- and -SO2-; R17 is absent or is C1-6 alkyl or an optionally substituted 5 to 12 membered carbocyclic or heterocyclic ring; provided that when R17 is absent, then L2 is also absent; and R2, R3, R4, R5, R11 and R’ are as defined in the claims. Compounds (I) modulate (PKA) and (PKB).
EP2647370A1 Transfusion preparation An object of the present invention is to provide an infusion preparation in which the Maillard reaction between an amino acid and a reducing sugar does not occur during storage and the size of fat particles in the fat emulsion does not increase during storage, and in which various types of vitamins can be incorporated in a stable manner, in spite of the fact that it is a two-chamber infusion preparation. Furthermore, even if only one of the infusions (of the infusion preparation) is administered, the patient is unlikely to develop hyperkalemia, vascular pain, or phlebitis. The present invention provides an infusion preparation containing two chambers separated by a partition that can be communicably opened, wherein a first chamber contains a first-chamber infusion containing a sugar and a fat emulsion, a second chamber contains a second-chamber infusion containing an amino acid and an electrolyte, the first-chamber infusion is substantially free of potassium, and has a relative osmotic pressure of 2.0 to 3.0, the second-chamber infusion has a potassium concentration of 40 mEq/L or less and a relative osmotic pressure of 2.5 to 3.5, and a mixture of the first- and second-chamber infusions has a potassium concentration of 16 mEq/L or more as measured upon communicably opening the partition.
CN101396356A New use of bilobalide The invention belongs to the medical field and in particular relates to the application of a ginkgolide in the preparation of a drug for remedying atherosclerotic thrombotic cerebral infarction and lacunar infarction. The experiment shows that the ginkgolide and the preparation thereof can provide the treatment of cardiovascular and cerebrovascular diseases, particularly the atherosclerotic thrombotic cerebral infarction and the lacunar infarction with clinical drugs with exact curative effect and high bioavailability.
US20110160128 Corin for Treating Obesity and Diabetes Provided herein are methods of inhibiting agouti or agouti-related protein (AGRP) in a cell or in an individual in need thereof, comprising administering to the cell or the individual an effective amount of an agent that induces corin expression, activity or a combination thereof in the cell or individual. The invention also provides a method of treating obesity in an individual in need thereof comprising administering to the individual an effective amount of an agent that enhances corin expression, activity or a combination thereof in the individual. Further provided is a method of treating diabetes type II in an individual in need thereof comprising administering to the individual an effective amount of an agent that enhances corin expression, activity or a combination thereof in the individual.
EP1311238B1 Use of di-sugar alcohol phosphates to protect human skin cells from uv-and/or ir radiation The invention relates to the incorporation of di-sugar alcohol phosphates of C3 to C6 sugar alcohols and/or derivatives of said compounds, e.g. acids, salts, or esters, into cosmetic or dermatological formulations for protecting the skin against environmental influences. The inventive low-molecular compounds of this type take part in the active cell protection of the cells' own free-radical scavengers, antioxidants, DNA, cell membranes and other cell compartments, protecting them against harmful environmental influences, e.g. UV radiation, IR radiation and environmental stress (thermal, chemical and physical). The compatible solution can act as a co-solvent and intensify the penetration of other active ingredients added to the cosmetic formulation, not only to stabilise said ingredients in the formulation, but also to actively transport them into deeper dermal layers.
US7423170 Anticancer agents based on regulation of protein prenylation Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.
US20080095850 produces homogeneous, free flowing, attrition resistant, uniform sized granules of etoricoxib for treating pain and inflammation in patients that cannot swallow a tablet The invention encompasses a process for granulating particles that produces homogeneous, free flowing, attrition resistant, uniform sized granules. When utilized with active pharmaceutical ingredients, such granules can be further processed into controlled released or taste-masked pharmaceutical formulations. Particularly, the process can be utilized to make an oral granule formulation of etoricoxib for treating pain and inflammation in patients that cannot swallow a tablet, such as young children and the elderly.
CN102688256A Liquid medicine for treating dental ulcer The invention discloses a liquid medicine for treating dental ulcer, and a preparation method of the liquid medicine; the liquid medicine comprises the components by volume percent: 10% of hydrochloric acid and 90% of distilled water, and the preparation method comprises the steps of: mixing 10ml of hydrochloric acid and 90ml of distilled water, shaking up and obtaining the liquid medicine for treating dental ulcer. The liquid medicine has the functions of resisting infection, diminishing inflammation, sterilizing and the like, can be used for treating various dental ulcer diseases, and is good in treatment effect, rapid in effect and convenient to use.
WO2008079993A3 Combinations of nitric oxide and sulfide and methods of use and manufacture thereof The present invention provides methods of reducing the cytotoxic effects of nitric oxide and sulfides comprising coadministering nitric oxide with sulfide. In addition, the present invention provides novel pharmaceutical compositions comprising both nitric oxide and sulfide. The methods and compositions of the present invention may be used in the treatment or prevention of a variety of diseases and disorders, and also in the prevention of cell or tissue damage, including that resulting from ischemia or hypoxia.
US20110196040 Skin Penetration Enhancing Systems for Polar Drugs The invention relates to pharmaceutical compositions and related methods for the topical administration of polar drugs. In a particular embodiment, the invention relates to a pharmaceutical composition comprising an active pharmaceutical agent that is a polar drug, such as potassium 2,5-dihydroxybenzenesulfonate, at least one occlusive agent, and at least one stabilizer.
US8394799 Compounds that inhibit HIF-1 activity, the method for preparation thereof and the pharmaceutical composition containing them as an effective component Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.
CN102030766B Flomoxef antibiotic containing pyrrolinheterocycle The invention belongs to the technical field of medicines, in particular to a flomoxef antibiotic containing pyrrolinheterocycle, shown in a general formula (I), or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, X, Y and n are defined in the specification. The invention also relates to preparation methods of the compounds, a medicine composition containing the compounds, and applications of the compounds to preparing medicines for treating and/or preventing cephalosporins sensitive diseases, especially infectious diseases.
WO2010102095A2 Kinase protein binding inhibitors The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating a variety of diseases and disorders, including cell proliferative disorders, especially cancer.
EP1328254B1 Lipid formulations for target delivery The present invention provides lipid-based systemic delivery vehicles and method for selectively targeting an active agent to a specific tissue site. The methods include designing a lipid-based systemic delivery vehicle having a plurality of constitutent parts, and thereafter varying the amounts of each of the plurality of constituent parts to impart tissue selectivity. After tissue selectivity is imparted it is possible to selectively target an active agent to a specific tissue site.
WO2011002525A1 Methods for treatment of muscular dystrophy The present invention relates to methods and agents useful for treating muscular dystrophy. Methods and agents for treating various physiological and pathological features associated with muscular dystrophy are also provided.
EP2575773A2 Synthetic nanocarrier combination vaccines Disclosed are dosage forms and related methods, that include a first population of synthetic nanocarriers that have one or more first antigens coupled to them, one or more second antigens that are not coupled to the synthetic nanocarriers, and a pharmaceutically acceptable excipient.
EP2560974A1 Pyrrazolopyridine derivatives The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, benzyl, -C(0)-lower alkyl, -C(0)-CH2-lower alkoxy, -C(0)-C3-6-cycloalkyl, -(CH2)°-C(0)-NR,R', -(CH2)°S(0)2- lower alkyl or -S(0)2-NR,R'; o is 0 or 1; R,R' are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a 5 or 6 membered heterocycloalkyl ring; R2 is hydrogen or lower alkyl; R3 is halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; and may be the same or different in case n is 2; n is 1 or 2; Ar is phenyl optionally substituted by one or two substituents selected from lower alkyl, halogen, lower alkoxy, lower alkyl substituted by hydroxy or cyano, or is a five or six membered heteroaryl group, selected from thiophenyl or pyridinyl which are optionally substituted by lower alkyl or halogen; or to a pharmaceutically active acid addition salt. It has surprisingly been found that the compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.
CN1830960B 10-phenyl hydroisoindolone type compounds, preparation method and use thereof A 10-phenyl hydroisoindolone compound is prepared from the spicaria elegans KLA03 extracted from marine specimen, and can be used as the cell reproduction inhibitor or antineoplastic medicine. Its preparing process is also disclosed.
US6927231 and stress-related degenerative processes associated with aging or diseases such as cancer, neurodegenerative disease or dysregulation of redox-regulated physiological processes, indicated by prooxidative shift in plasma thiol/disulfide redox state The present invention relates to a method of amelioring oxidative stress and stress-related degenerative processes associated with aging or various disease conditions such as cancer, neurodegenerative diseases or the dysregulation of redox-regulated physiological processes, as indicated by the prooxidative shift in the plasma thil/disulfide redox state and its consequences in conditions of elevated oxidative stress, characterized by administering creatine.
WO2007071691A1 3- (4-{ [4-(4-{ [3-(3, 3-dimethyl-1-piperidinyl) propyl] 0xy} phenyl) -1-piperidinyl] carbonyl }-1-naphthalenyl) propanoic or propenoic acid as h1 and h3 receptor antagonists for the treatment of inflammatory and/or allergic disorders The present invention relates to a compound of formula (I), or a salt thereof wherein the naphthalene ring can be substituted in the 2, 3, 4, 5, 6, 7 or 8 position by R1, and R1 represents -CH2CH2COOH or -CH=C(CH3)COOH, and to processes for their preparation, to compositions containing them and to their use in the treatment of various diseases such as allergic rhinitis.
EP0938315B1 Immune response modifier compounds for treatment of th2 mediated and related diseases Immune response modifier compounds - imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, and 1,2-bridged imidazoquinoline amines - are useful for the treatment of TH2 mediated diseases by administering a therapeutically effective amount of such compounds in order to inhibit TH2 immune response, suppress IL-4/IL-5 cytokine induction and eosinophilia, as well as enhance TH1 immune response.
CN101940635B Nanometer ceanothus bismuth magnesium tablet and preparation method thereof The invention discloses a nanometer ceanothus bismuth magnesium tablet and a preparation method thereof. The preparation method is characterized in that bismuth subnitrate is synthetized by adopting a hydro-thermal method to prepare the nanometer ceanothus bismuth magnesium tablet and comprises the following steps of: firstly, dissolving bismuth oxide and nitric acid into a proper amount of glycol to prepare a saline solution; secondly, dripping the saline solution into a hartshorn, and stirring to obtain a precipitate after titration; thirdly, repeatedly cleaning and ageing the precipitate with purified water to prepare a hydro-thermal reaction precursor solution; fourthly, adding the precursor solution and a mineralizer into a hydro-thermal reaction kettle, reacting for a period of time, taking out a product in the reaction kettle, washing the product with the purified water to obtain a white crystalline substance, cleaning the white crystalline substance with absolute ethyl alcohol, and drying at the room temperature to obtain bismuth subnitrate powder; fifthly, preparing the nanometer ceanothus bismuth magnesium tablet by 300g of the bismuth subnitrate synthetized through the hydro-thermal method, 200g of sodium bicarbonate, 400g of magnesium carbonate, 25g of Frangula alnus, pharmaceutically acceptable adhesives and auxiliary materials. The invention has the advantages ofsimple process control, rapid disintegration and high bioavailability.
US20110172290 Isoforms of eIF-5A: Senescence-induced eIF5A; Wounding-induced elF-5A; Growth elF-5A; and DHS The present invention relates to unique isoforms of eukaryotic initiation Factor 5A (“eIF-5A”): senescence-induced eIF-5A; wounding-induced eIF-5A; and growth eIF-5A, as well as polynucleotides that encode these three factors. The present invention also relates to methods involving modulating the expression of these factors. The present invention also relates to deoxyhypusine synthase (“DHS”), polynucleotides that encode DHS, and methods involving modulating the expression of DHS.
US20100330101 BIFUNCTIONAL CpG OR OLIGO-/POLYNUCLEOTIDE AND TOXIN OR ENTEROTOXIN CONTAINING COMPOSITION A bifunctional composition comprising an intracellularly effective immunomodulating nucleic acid component containing at least one immunostimulatory, immunoinhibitory or immunomodulating motif and selected from a mononucleotide, a dinucleotide, an oligonucleotide or a polynucleotide with either a natural phosphodiester backbone or a modified backbone, optionally in combination with a specific antigen, in association with a protein binding to specific receptors on mammalian cell surfaces selected from the group consisting of cholera toxin (CT), the subunit B of CT (CTB), Escherichia coli heat labile enterotoxin (LT), the subunit B of LT (LTB), and proteins or protein derivatives that react with antiserum to CT or LT, bind to GM1 ganglioside, ADP-ribosylates an acceptor protein, or give rise to accumulation of cyclic AMP in target cells, and antibodies or other proteins which after binding to a specific cell surface component can be internalized into the cell, is described. The composition is useful for treatment of tumors, infections, graft rejections, immunosuppressive states, autoimmune diseases and allergies, and further with a specific antigen it is useful for immunoprophylaxis, immunotherapy or induction of tolerance, and for treatment ex vivo of an antigen-presenting cell for subsequent infusion into a mammal for vaccination or immunotherapy purposes.
CA2320731C Antibiotics in dry dosage forms for the treatment of shallow ulcers of the oral mucosa The invention provides a medicament for topically treating aphthous ulcers in the oral mucosa, and methods of use. The medicament Ii comprises a troche or powder comprising a dry dosage of one or more antibiotics and, preferably, one or more polyvalent metal compounds.The troche or powder is directly applied to the aphthous ulcer and dissolves in saliva, within about 5 to about 15 minutes, thereby directly delivering a supratherapeutic dosage of the antibiotic to the ulcerated oral tissue. Further, in a preferred embodiment the troche/powder directly delivers a therapeutically high concentration of a polyvalent metal compound in suspension to the aphthous ulcer, thereby forming a protective barrier over the ulcerated oral tissue.
WO2008003484A3 Agent containing chrysin and cholic acid for reducing weight, accelerating lipid catabolism, and/or restricting calories Disclosed is the use of a preparation comprising chrysin and cholic acid for producing a medicament that is utilized for reducing weight, accelerating lipid catabolism, and/or restricting calories.
CN1634859A Symmetrel derivatives and synthesis method thereof and their use as neuron damage protective agent The invention relates to symmetrel derivatives and their synthesis process and use as neuron damage protector. Said symmetrel derivatives are N-alkyl monosubstituted, N-alkyl disubstituted and N-acidylated derivative of symmetrel compounds. In vitro experiment shows that the tested compounds can make the growth of damaged neuron SY5Y normal under condition of some concentration.
US7262186 Kinesin spindle protein inhibitor; antiproliferative agents; anticancer agents; 4-(2,5-difluorophenyl0-N-3-fluoropyrrolidin-3-yl)-2-hydroxymethyl-2-phenyl-2,5-dihydro-1N-pyrrol-1-carboxamide The present invention relates to azolopyriniidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
US7435750 Method of using substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
US20100120859 Novel case of renin inhibitors The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups, and their use in treating cardiovascular events and renal insufficiency.
CN101584798A A chinese midicine for curing psoriasis completely The invention relates to a chinese midicine for curing psoriasis completely, its components include: erythromycin, vanishing cream, fluocinolone acetonide, cigarette oil, dry artemsia argyi, garlic core, which can not only cure psoriasis effectively without recrudescence, but also the medication is simple with obvious effects and without any toxic side effect, the curing ratio is approaching 94% and the price is low, which is particularly siutable for vast rural areas in shortage of medical services and medicines.
CN102552151A Preparation technology of aztreonam for injection The invention provides a preparation technology of aztreonam for injection. The formula comprises aztreonam and arginine. The preparation technology comprises the following steps of: cleaning and sterilizing a penicillin bottle, a butyl rubber plug and an aluminum-plastic cover; and sub-packaging.
US20100260743 Solubilization and Targeted Delivery of Drugs With Self-Assembling Amphiphilic Polymers There are provided amphiphilic biodegradable copolymers comprising a hydrophilic backbone with pendant aliphatic groups as the hydrophobic component. The polymers form nanoscale molecular aggregates in aqueous environments, which have hydrophobic interiors that are capable of solubilizing insoluble organic compounds such as drugs, vitamins, dyes, and imaging agents. The polymers optionally feature reactive functional groups that provide attachment points for antibodies, ligands, and other targeting moieties useful for the targeted delivery of drugs and imaging agents.
US20090048151 PEG-Poly(Ortho Ester) Graft Copolymers and Pharmaceutical Compositions This invention relates to graft copolymer delivery vehicles comprising a polyethyleneglycol-poly(ortho ester), and to controlled release pharmaceutical compositions comprising the delivery vehicle and an active agent. The graft copolymer delivery vehicles may be thermogels graft copolymers. The pharmaceutical compositions may be in the form of a topical, syringable, or injectable formulation for local controlled delivery of the active agent.
US7700554 Compositions for modulating blood-brain barrier transport This invention provides conjugates of therapeutic or active agents with melanotransferrin or with other ligands of a melanotransferrin receptor, melanotransferrin receptor modulators, and related compositions and methods for modulating blood-brain barrier transport by providing methods of screening and selecting such conjugates, ligands, and modulators in vitro and in vivo, and methods of use of such conjugates, modulators and ligands in diagnosis and the treatment of diseases, including particularly diseases of the central nervous system or lysosomal storage diseases.
CN103725552A Herba Polygalae Japonicae health liquor used for tonsillitis The invention relates to a Herba Polygalae Japonicae health liquor used for tonsillitis. The Herba Polygalae Japonicae health liquor is prepared through a step of washing 18g of Herba Polygalae Japonicae, 13g of Herba Verbenae, 11g of borneol, 14g of dragon's blood, 14g of dried orange peel and 15g of dahurian angelica root, a step of air-drying, a step of crushing to form powder, a step of immersing the powder in 1000g of a white liquor at normal temperature for 24-34 days, a step of filtering the above immersed material, a step of taking the above obtained filtrate, and a step of mixing the filtrate with 3500g of wine. The Herba Polygalae Japonicae health liquor used for tonsillitis has the advantages of simple preparation method and drinking convenience, has the efficacies of yin nourishing, dryness moisturizing, hardness softening and bind dissipating, and can be frequently drunk to realize the yin nourishing, dryness moisturizing, hardness softening, bind dissipating and the body resistance of people in order to prevent and treat the tonsillitis.
WO2011101409A1 Pyrrolopyrimidine compounds as inhibitors of cdk4/6 The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8- R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
CN102885865A Antiallergic tablet The present invention relates to an antiallergic tablet, and belongs to the technical field of pharmaceuticals. The composition of the tablet includes: loratadine, sodium dodecyl sulfate, starch, microcrystalline cellulose, vitamin C, povidone, borneol, angelica, talc powder and poria. The tablet is prepared by mixing, heating, condensing, drying, and sizing. The product of the present invention has a good antiallergic effect, can cure various allergy symptoms caused by foods and contacts, also can be applied to chronic measles, psoriasis and the like, and produces a significant effect by taking. No harmful chemical substances are added in the preparation process, no side effects generated after use, the production process is simple, the cost is low, and the tablet is suitable for promotion and application.
EP1565438B1 Antitumor benzoylsulfonamides The present invention provides antitumor compounds of the formula (I); and antitumor methods.
EP2474552A1 New saccharide mimics and their use as inhibitors of angiogenesis and metastasis formation The present invention relates to saccharide mimics which show a better biological activity at low concentrations as known saccharide mimics in inhibiting angiogenesis and inhibiting formation of metastasis by inhibiting adhesion and/or migration of human cancer cells, particularly in concentrations lower than 5 mM, and to pharmaceutical compositions comprising these saccharide mimics. The compounds of the present invention are useful as mimics of cell surface structures and, thus, for influencing cell-cell and cell-extracellular (ECM) interactions, which are controlled by bonds between protein-protein, saccharide-saccharide or saccharide-lectin on the cell-surface. Representative compounds of the present invention are for example:
CN103479817A Wound healing gel The invention discloses a wound healing gel. The wound healing gel comprises the following components by weight: 30-40 parts of erythromycin, 3-10 parts a phellodendron extractive, 5-10 parts of a rhubarb extractive, 2-5 parts of a mulberry leaf extractive, 5-10 parts of an Aloe vera extractive, 10-20 parts of carbomer, 2-5 parts of triethanolamine, 3-6 parts of polyvinyl pyrrolidone and 15-20 parts of glycerol. The gel provided by the invention has efficacies of heat clearing, detoxifying, cooling, refreshing, relieving pain, removing slough, promoting growth of tissue regeneration, astringing wound, reducing postoperative wound infection and postoperative complications, can treat trauma and wound infections. The gel has the advantages of easiness for absorption, good curative effect, no scar, simple processing method, no toxic or side effect, simple and practicable preparation technology, cheap and abundant drug sources, low cost and high benefits.
US6855709 Psychological disorders; central nervous system disorders The invention provides compounds of the formula and methods of using those compounds for treating a disease or condition in a mammal wherein a 5-HT receptor, such as a 5-HT6 receptor, is implicated and modulation of a 5-HT function is desired, wherein A, G and W1-W3 are defined as herein.
EP0975223B1 In-situ generation of zinc pyrithione Disclosed is a personal care composition comprising: (a) water or an alcohol, (b) at least one dispersant or surfactant, and (c) as an antimicrobial or preservative additive, particles of an in-situ transchelation reaction product of a zinc compound selected from the group consisting of zinc salts of organic acids, zinc salts of inorganic acids, zinc hydroxide, zinc oxide, and combinations thereof, said zinc compound being soluble in said water or alcohol, with pyrithione acid or a pyrithione salt that is soluble in said water or alcohol. Also disclosed is a process for preparing the personal care composition, and a coated substrate containing a coating of the personal care composition.
WO2008072072A1 Terminally unsaturated vanilloids and medicinal application thereof Terminally unsaturated vanilloids for the manufacturing of a medicinal composition to treat capsaicin-responsive conditions. Said vanilloids are devoided of the disadvantage of capsaicin and analogs, namely the discomforting pungency, while retaining several of the their biological and clinically useful properties.
WO2008142397A1 Serine protease inhibitors for use in the treatment of bacterial infections Use of a serine protease inhibitor selected from camostat, the metabolite of camostat, gabexate, nafamostat or sepimostat, or a pharmaceutically acceptable salt thereof, as an inhibitor of pathogenic bacterial growth.
WO2010011619A1 Large substituent, non-phenolic amine opioids 8-Substituted-2,6-methano-3-benzazocines of general structure (I) are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
US8741912 Deazapurines useful as inhibitors of Janus kinases The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The compounds are generally represented by structural formula I or pharmaceutically acceptable salts thereof:
US20100261788 Inhibition of Bid-Induced Cell-Death Using Small Organic Molecules Various phenylamine derivatives are described as well as the use of compounds to inhibit BID protein for controlling apoptotic cascade.
CN103705576A Medicinal composition for preventing and treating mycotoxicosis of pigs, as well as preparation method and application thereof The invention discloses a medicinal composition for preventing and treating mycotoxicosis of pigs, as well as a preparation method and application thereof. The medicinal composition comprises the following components in percentage by weight: 8-14 percent of germanium amino acid chelate, 40-80 percent of salvia extract, and the balance of auxiliaries, wherein the germanium amino acid chelate comprises but is not limited to germanium lysine, germanium methionine, germanium hydroxymethionine, germanium glycine, germanium tryptophane, germanium threonine and the like. The medicinal composition is scientific in compatibility, low in cost and convenient to use, has the effect of promoting metabolism of mycotoxin in a pig body and treating immunosuppressive diseases of a pig, can be directly added in pig feed and drinking water, does not have toxic or side effect or drug residue, is a medicinal composition which accords with safe veterinary drugs, guarantees animal-derived food safety for preventing and treating mycotoxicosis.
US7709449 Treating hepatitis infections, particularly hepatitis B viral infections; modified oligonucleotides The invention provides compounds capable of treating against hepatitis infections, particularly hepatitis B viral infections. Compounds of the invention are nucleic acid-based and preferably comprise 2, 3, 4, 5 or 6 nucleoside units.
WO2011029404A1 Mir-125a for regulating expression of rantes, composition and use thereof The invention provides the use of miR-125a for manufacturing the substance for treating the diseases mediated by inflammatory chemokine RANTES, the pharmaceutical composition comprising miR-125a, the method for regulating expression of RANTES in tissues or cells using miR-125a in vitro, and the method for screening the substance with capability of regulating the expression of RANTES.
CN101724008A Marsdenia tenacissima C21 steroidal glycoside converted product and preparation method and application thereof The invention provides a marsdenia tenacissima C21 steroidal glycoside converted product and a preparation method and application thereof. The content in percentage by weight of marsdenia tenacissima C21 steroidal glycoside contained in the converted product is larger than or equal to 50 percent, wherein the content in percentage by weight of 11alpha-O-tigloyl-12beta-O-acetyl-tenacigenin B is larger than or equal to 6 percent. The invention also discloses the preparation method of the marsdenia tenacissima C21 steroidal glycoside converted product and the application thereof to preparing a medicament for preventing and/or treating digestive tract tumors.
WO2009118371A1 Use of nicotinamide for treating summer itch in horses The present invention relates to the use of nicotinamide, as pure nicotinamide or in the form of vitamin B3, for the treatment of summer itch in non-human mammals such as horses and cattle.
US20080064690 Neuropathic or inflammatory pain relief; inhibiting ion flux through channel including PN3 subunit; potency Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides pyrazole-amides and -sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.
CN102030700A Benzamide carboxylic acid compound as well as manufacturing method and medicinal application thereof The invention discloses a new benzamide carboxylic acid compound of formula I, an enantiomer, a racemate and physiologically acceptable salt, solvate and crystalline form thereof, a preparation method of the compound, a medicinal preparation containing the compound and an application of the compound in clinic treatment related to insulin resistance.
CN102766135A Dihydrofuran indenoane-imidazole salts compound and preparation method thereof The invention discloses a series of dihydrofuran indenoane-imidazole salts compounds and a preparation method thereof. The preparation method comprises the following steps of: carrying out Vilsmeier reaction and Perskin reaction on 2,3-dihydrobenzofuran taken as a raw material; reducing palladium/carbon in an acetic acid to 5-propionic acid dihydrobenzofuran and forming acyl chloride with thionyl chloride; carrying out intramolecular Friedel-Crafts reaction and reducing in an alcohol solution by using sodium borohydride to obtain dihydrofuran indenoanol; forming a chloride in a toluene solution with the thionyl chloride; and reflowing and reacting with imidazole or 2-methyl imidazole or 2-ethyl imidazole or benzimidazole in acetonitrile or a toluene solvent to synthesize 1-(dihydrofuran indenoane) imidazole, and reacting with a halide on the above basis to synthesize the compound. According to the dihydrofuran indenoane-imidazole salts compounds and the preparation method thereof, pharmacophores with obvious tumor resisting activity in natural products are used as precursors to carry out designing and synthesizing on anti-tumor medicine molecule, and when an imidazole structure unit in a synthesized compound is the benzimidazole, particularly a naphthoyl methyl imidazole salts compound, the compound has very good in-vitro anticancer physiological activity.
WO2006063791A1 3-benzylthio-1,2,4-triazine-5 (2h)-one as paf-ah inhibitors The invention relates to 3-benzylthio-1,2,4-triazine-5 (2H)-one of formula I, methods for the production thereof, and the use thereof for producing medicaments that are used for the treatment and/or prevention of diseases, especially chronic inflammatory diseases, such as diseases of the rheumatic type, and cardiovascular diseases, e.g. dyslipidemia, arteriosclerosis, and coronary heart diseases.
EP0815204B1 Method for treating tumors by alloactivated human donor lymphocytes A method is provided for treatment of a mammalian patient having a tumor by administering to the patient allogenic donor lymphocytes that have been co-cultured in the presence of the patient-derived lymphocytes under conditions sufficient to alloactivate the donor lymphocytes. It is preferred that the donor lymphocytes be introduced intralesionally. This method is preferred for treatment of glioblastoma in humans.
CN103142506A Cefpodoxime proxetil granules and preparation method thereof The invention relates to cefpodoxime proxetil granules and a preparation method thereof. The granules comprise the following components in parts by weight: 40-60 parts of cefpodoxime proxetil, 700-950 parts of filler, 30-50 parts of disintegrant, 30-50 parts of binder, 12-35 parts of flavoring agent, 2-10 parts of disintegration promoting agent and 1-7 parts of other auxiliary materials. The preparation method of the granules specifically comprises the following steps of: (1) performing pretreatment on the raw materials and the auxiliary materials; (2) mixing; (3) performing granulation; and (4) performing total mixing. The cefpodoxime proxetil granules prepared by the preparation method disclosed by the invention have the advantages of capability of obviously reducing the bitterness of the raw materials, stable preparation, controllable quality, good medicament dissolution and higher safety and effectiveness in clinical medication, and is suitable for industrial mass production and the like.
WO2006060884A1 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]decanes The present invention relates to 7-(2-cyclohexylidene-ethylidene)- spiro[4.5]-decanes, compositions which comprise said 7-(2-cyclohexylidene- ethylidene)-spiro[4.5]-decanes, and methods for treating diseases, illnesses, and the like with said 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]decanes.
US20100069313 Novel powders based on vegetation water from olive oil production The present invention is directed a process for the manufacture of a powder comprising vegetation water rich in water-soluble polyphenols, especially rich in hydroxytyrosol, as well as to the powders themselves and dietary supplements, especially in form of tablets, food, feed and cosmetic preparations containing such powders. The process comprises the following steps: A) providing vegetation water (concentrate) containing water-soluble polyphenols; B) (optionally) modifying the water content of the vegetation water (concentrate); C) optionally centrifuging the vegetation water (concentrate) and separating the water-soluble part; D) spray-drying or granulating the (water-soluble part of the) vegetation water (concentrate), preferably in presence of an adjuvant; E) optionally washing the thus obtained powder comprising vegetation water rich in water-soluble polyphenols with an organic solvent.
US7696194 Visual function disorder improving agents The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent has axon of the retinal ganglion cellal extension promoting action and optic nerve cell regeneration promoting action, and is useful for the treatment of a visual function disorder associated with various eye diseases caused by damage, defects, degeneration and the like in the retinal or optic nerve.
CA2174098C Method of inducing and maintaining neuronal cells The present invention makes available a method for inducing neuronal differentiation and preventing the death or degeneration of neuronal cells both in vitro and in vivo. The subject method stems from the unexpected finding that, contrary to traditional unterstanding of neural induction, the default fate of ectodermal tissue is neuronal rather than mesodermal and/or epidermal. In particular, it has been discovered that preventing or antagonizing a signaling pathway in a cell for a growth factor of the TGF-.beta. family can result in neuronal differentiation of that cell.
US20100291226 Pharmaceutical Formulations Based on Apolar and Polar Lipids for Ophthalmic Use The present invention refers to pharmaceutical formulations based on lipids for ophthalmic use comprising a phospholipid component composed of zwitterionic phospholipids of natural origin and an oily component composed of oils of natural origin emulsified in water. In particular, the invention refers to ophthalmic formulations useful, for example, for transporting drugs to the eye and in the treatment of ocular dryness, capable of restoring the lipid layer of the tear film. In particular, in a non-transitory but pathological situation such as the dry eye syndrome, such formulations also succeed in reducing the often-present inflammatory component.
EP1341778B1 Klainetin and derivatives thereof, method for their production and the use of the same The invention relates to compounds of general formula (I): and formula (II): wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, X5 and Y are defined as per the description. The compounds of formula (I) and (II) inhibit cyclin-dependent kinases (CDKs) and additional kinases (KDR), have cytostatic properties and are particularly suitable for treating tumours. The compounds of formulas (I) and (II) can be obtained by extraction of the plant Uvaria klaineri, PLA 100484, by cell cultures of the plant Uvaria klaineri or by chemical synthesis. The invention also relates to a method for producing the compounds of formulas (I) and (II), to the use of said compounds for producing a medicament for treating malignant diseases and diseases that can be treated by inhibiting CDKs and KDR.
EP1036083B9 Novel 9a-azalides The invention relates to compounds of general formula (I) characterized in that R1 individually stands for hydroxyl, L-cladinosyl group of formula (II) wherein R2 individually stands for hydrogen or a silyl group; R3 individually stands for hydrogen or together with R6 stands for an ether group; R4 individually stands for hydrogen, (C1-C4)acyl group or -COO-(CH¿2?)n-Ar group, wherein n is 1-7 and Ar individually stands for unsubstituted or substituted aryl group with up to 18 carbon atoms; R?5¿ individually stands for hydrogen, methyl group or -COO-(CH¿2?)n-Ar group, wherein n is 1-7 and Ar individually stands for unsubstituted or substituted aryl group with up to 18 carbon atoms; R?6¿ individually stands for a hydroxyl group or together with R3 stands for an ether group; R7 individually stands for hydrogen, (C¿1?-C12)alkyl group, silyl group or together with R?8¿ and C-11/C-12 carbon atoms stands for a cyclic carbonate, R8 individually stands for hydrogen, (C¿1?-C12)alkyl group, silyl group or together with R?7¿ and C-11/C-12 carbon atoms stands for a cyclic carbonate; and its pharmaceutically acceptable additions salts with inorganic or organic acids, to a process for the preparation thereof and to the use thereof as antibiotics or as intermediates for the synthesis of other macrolide antibiotics.
CN1827095A Pharmaceutical composition using pregabalin as active ingredient, its preparation method and use This invention is about a medicine composition taking prinebalyn as active component and its preparing method and usages. It takes prinebalyn as medicine active component, and is formed by mixing acceptable finding. It is used to cure outer neuralgia and grand partly epilepsy. It uses prinebalyn as raw material and adds some findings those have specified kinds and ratios. Developing troche, capsule, dispersing tablets, granula, soft capsule, chewing tablets, buccal tablets, droplet, and other oral preparations according to the method in this invention.
CN101983964A Compound with antibacterial activity and antitumor activity and preparation method and applications thereof The invention relates to the microbial field and discloses a compound generated by a microorganism and a preparation method and applications thereof. The structural formula of the compound is shown in the formula I. The invention also provides the microorganism used for producing the compound, wherein the microorganism is preserved in the China General Microbiological Culture Collection Center and has the preservation number of CGMCCNo.3629. The compound of the invention has antibacterial activity and antitumor activity, and can be used to prepare medicines for curing bacterial infection and tumor and have wide clinical application prospect.
CN102949442A Medicinal composition for oral hygiene and disinfection and preparation method thereof The invention discloses a medicinal composition for oral hygiene and disinfection and a preparation method of the medicinal composition. The medicinal composition contains the following components in parts by weight: 10 parts of menthol, 1 part of borneol, 1 part of mint essence, 16 parts of ethanol and 72 parts of distilled water. According to the invention, the medicinal composition is expected to reach the effects of the oral hygiene and disinfection, and is prepared by the menthol, the and the mint essence as the main raw materials based on a scientific and reasonable production technology. The product is definite in function, controllable in quality and safe to take. According to the invention, the preparation method of the medicinal composition is simple, and the preparation of the medicinal composition can be finished by conventional equipment.
WO2010146351A1 Indolylmethyl-morpholine derivatives as kinase inhibitors A series of morpholine derivatives, substituted in the 4-position by a substituted carbonyl or sulfonyl moiety, and in the 3-position by an optionally substituted indol-3-ylmethyl group, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
WO2013104611A1 Substituted pyrazolopyrimidines as akt kinase inhibitors Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
WO2010078916A4 Immunocytokines for tumour therapy with chemotherapeutic agents lmmunocytokine comprising cytokine, e.g. interleukin 2 (IL-2), conjugated to antibody against tumour neovasculature antigen, e.g. tenascin-C, for use in combination therapy with chemotherapeutic agent such as temozolomide. Use of immunocytokine and chemotherapy for treatment of tumours e.g. glioblastoma and other cancers.
CN101439188A Polymer lyophilized preparation of insoluble anti-tumor medicament The invention discloses a polymer freeze-dried preparation of a poorly soluble anti-tumor drug, and the polymer freeze-dried preparation is prepared by the following method: (1) weighing the poorly soluble anti-tumor drug, cyclodextrin, polyethylene glycol, polyether F-68, polyol, trehalose and bile salt; (2) the poorly soluble anti-tumor drug and the polyether F-68 are dissolved in anhydrous ethanol, and are evaporated till no ethanol is evaporated; (3) the cyclodextrin, the polyethylene glycol, the polyol, the trehalose and the bile salt are added into water for injection for preparing polymer solution; (4) the polymer solution is mixed with products obtained by the step (2), and uniform and transparent solution is obtained by stirring; (5) the filtration by a microporous filtration membrane is carried out to obtain the uniform and transparent solution; (6) and the freeze-drying is carried out to obtain the polymer freeze-dried preparation of the poorly soluble anti-tumor drug. The polymer freeze-dried preparation of the poorly soluble anti-tumor drug can greatly improve the solubility of the poorly soluble drug in water solution, the operation is simple and convenient, the organic residues are fewer, and the stability of the preparation product is high.
CN102846768A Preparation process of integration-type novel formulation of Radix Et Rhizoma Rhei and Paeonia suffruticosa decoction and production method thereof The invention relates to a preparation process of integration-type novel formulation of Radix Et Rhizoma Rhei and Paeonia suffruticosa decoction and a production method thereof. The effective components of the novel formulation are made from the following raw materials (by weight parts): Radix Et Rhizoma Rhei 18, Paeonia suffruticosa bark 9, Semen Persicae (Prunus persica and/or Prunus davidiana) 12, Benincasa hispida seed 30 and mirabilite 9. The production method includes the steps of supersonic airstream pulverization, alcohol-water extraction, ultrasonic pulverization and extraction, water decoction and concentration, supersonic spray-drying, nano-scale grinding, high-pressure emulsion and homogenization and nanoparticle preparation. The production method integrates the advantageous of the nano-carrier combination technique, such as multi-component synergism and multi-target. The large-scale production can greatly reduce the production cost, greatly improve the product quality and enhance the target property and sustained/controlled-release property of drugs. The novel formulation is administered by oral intake and external application during four time periods respectively based on the midnight-noon tidal flow and human qi-blood flow rule. The novel formulation is also processed to membranes and transdermal delivery agents which are applied to different parts of human body respectively according to the midnight-noon tidal flow and human qi-blood flow rule and can be directly absorbed by the skin.
US20080274169 Flexible, penetrating liposomal carrier system; bilayer of phospholipids, a hydrophobic photosensitizer, skin penetration enhancers; penetrating through an intact stratum corneum or wound surface without removal of photosensitizer from bilayer without agglomeration of bilayers Highly flexible penetrating liposomal carrier systems are formulated with enhanced skin penetration properties. These specialized formulations of highly flexible penetrating liposomal delivery systems comprise one or more phospholipids, lysophosphatides and hydrophobic photosensitizer. This new formulations can squeeze liposomal particles through intercellular regions of stratum corneum as intact structures, and, in this way, deliver encapsulated photosensitizer to the epidermis, dermis, hypodermis and surroundings. The penetrating liposomal formulation provides therapeutically effective amounts of the hydrophobic photosensitizer through topical application with better skin penetration thus improving drug targeting and the efficacy of photodynamic therapy (PDT).
CN101580821B 2-naphthoic monooxygenase for preparing anti-cancer medicament indigo red The invention discloses a 2-naphthoic monooxygenase, a mutant thereof, and use thereof in the biocatalytic preparation of anti-cancer drug indigo red. Experiments prove that 2-naphthoic monooxygenase can catalyze the indigo red generation of indole, that the modified molecular 2-naphthoic monooxygenase mutant can also be used in the biocatalytic preparation of indigo red, that the catalytic efficiency of the 2-naphthoic monooxygenase is higher than that of wild 2-naphthoic monooxygenase, and that the catalysis efficiency of the mutant is 2 to 4 times larger than that of the wild mutant. The 2-naphthoic monooxygenase is mainly used for biological preparation of the anti-cancer medicament indigo red.
US20100135981 Use of the endoglycosidase endos for treating immunoglobulin g mediated diseases The invention provides use of an EndoS polypeptide, or a polynucleotide encoding an EndoS polypeptide, in the manufacture of a medicament for the treatment or prevention of a disease or condition mediated by IgG antibodies.
US20100068229 Recombinant antigens of human cytomegalovirus (hcmv) The invention described herein relates to a method for identifying the antigenic regions of HCMV proteins involved in the human B-cell response to HCMV infection, for combining such antigenic regions in the form of chimeric fusion products, and their use as diagnostic and immunogenic agents.
US20130005689 Compounds for the treatment of addiction Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
CN101978961A Composition for treating gingivitis or peridentitis and application thereof The invention discloses a composition for treating gingivitis or peridentitis. The composition comprises the following components in part by weight: 0.2 to 0.5 part of amoxicillin (a), 0.1 to 0.4 part of metronidazole or tinidazole (b), 0.05 to 0.1 part of trimethoprim (c), and pharmaceutically and physiologically acceptable carrier (d). The composition has the advantage of effectively inhibiting or killing anaerobic bacteria and microaerophilic bacteria in the oral cavity, thereby quickly and effectively treating the gingivitis or the peridentitis.
WO2010125271A1 Use of n2o gas for treating chronic pain The invention relates to a gas mixture that contains nitrous oxide (N2O) for use as a breathable drug for the treatment of chronic pain in a mammal, in particular a pain from neuropathic, iatrogenic, dysfunctional or inflammatory origin, in particular in humans. The proportion of N2O ranges from 15 to 45 vol. %. The gas mixture is administered for a sufficient duration for obtaining a delayed pain hypersensitivity reduction that can be observed at least 6 hours after the end of the inhalation of the gas mixture by said mammal. The pain hypersensitivity is selected from allodynias and hyperalgesias.
US8535721 Pharmaceutical microspheres containing valproic acid for oral administration The subject of the invention is pharmaceutical microspheres containing, as active principle, a mixture of valproic acid and of one of its pharmaceutically acceptable salts in combination with a matrix vehicle selected from glycerol esters, hydrogenated oils, esterified polyethylene glycols, waxes and their mixtures.
CA2549029A1 Compositions for treatment or prevention of metabolic syndrome This invention concerns the use of an amine oxidase enzyme inhibitor for the manufacture of a pharmaceutical preparation useful in the treatment or prevention of metabolic syndrome and diseases or conditions resulting therefrom. The invention concerns also the use of vitamin B1 or a metabolite thereof for the manufacture of a pharmaceutical preparation useful as an amine oxidase enzyme inhibitor. Furthermore, the invention concerns a food product comprising an amine oxidase enzyme inhibitor in combination with a foodstuff, a food additive comprising an amine oxidase enzyme inhibitor in combination with a liquid, solid or semisolid carrier.
WO2013054146A1 New co crystals useful in the preparation of pharmaceutical compositions The invention relates to the new co crystals of 5-chloro-N-///5S/-2-oxo-3-/4-/3- oxo-moφholine-4-yl/-phenyl/-l,3-oxazolidine-5-yl/-methyl/-thiophen-2- carboxamide having the INN rivaroxaban formed with oxalic acid and gamma- cyclodextrine. The invention also relates to a process for the preparation of the co crystal of rivaroxaban and oxalic acid of the Formula 2. According to said process amorphous or crystalline rovaroxaban or a hydrate, solvate or co crystal of rivaroxaban is dissolved in an organic solvent, water or a mixture of an organic solvent and water, to the solution oxalic acid is added and the solvent is removed. According to the invention there is also provided a process for the preparation of the co crystal of rivaroxaban and gamma-cyclodextrin of the Formula 3 /wherein n is 0.9-1.1, preferably n=l/. According to said process amorphous or crystalline rivaroxaban or a hydrate, solvate or co crystal of rivaroxaban is dissolved in an organic solvent, water or a mixture of an organic solvent and water, to the solution gamma-cyclodextrine is added and the solvent is removed.
CN1837231A Immunomodulatory steroids, in particular the hemihydrate of 16, alpha-bromoepiandrosterone The invention provides compositions comprising formula 1 steroids, e.g., 16alpha-bromo-3beta-hydroxy-5alpha-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16alpha-bromo-3beta-hydroxy-5alpha-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
CN103263392A Amoitone derivative long-circulation nanometer lipid carrier and preparation method thereof The invention discloses an amoitone derivative long-circulation nanometer lipid carrier which comprises the following main components: crude medicine Amoitone B, polyoxyethylene glycol bisstearate, solid lipid material, liquid lipid material, fat-soluble emulsifier, water-soluble emulsifier and injection water. The preparation method of the amoitone derivative long-circulation nanometer lipid carrier is an emulsion evaporating-low temperature curing method. The amoitone derivative long-circulation nanometer lipid carrier prepared by the preparation method has a slow release function in the body, is capable of effectively prolonging the in-vivo retention time of the medicine and improving the bioavailability of the medicine, has higher encapsulation efficiency and medicine carrying amount and a grain size of about 200nm, and can be passively targeted to a liver tissue, so that the toxic and side effects of the Amoitone B are lowered. Moreover, the amoitone derivative long-circulation nanometer lipid carrier is good in biocompatibility, easy to degrade, good in stability and capable of improving body tolerance and patient compliance.
WO2011133010A3 Molecular iodine composition for human use for the prevention and treatment of prostatic pathologies The invention relates to a pharmaceutical composition for preventing and treating prostatic pathologies in humans such as benign prostatic hyperplasia (BPH) or prostate cancer. The composition is characterised in that it contains between 3 and 10 mg of molecular iodine as the active substance, combined with pharmaceutically acceptable excipients and can be prepared in an oral form (tablets, solution or drops) and in a topical form (gel or delayed release patch). The composition also has a cardioprotector effect when used as an adjuvant with anti-cancer drugs such as anthracyclines.
EP1385505B1 Acne treatment with lipooxigenase inhibitors The invention relates to the use of lipooxigenase inhibitors for treating acne, particularly inflammatory acne. The inventive lipooxigenase inhibitor can be used alone or in combination with other lipooxigenase inhibitors or anti-acne active agents in a pharmaceutically suitable composition, particularly through oral and/or local-topic application.
CN1973819A Anticancer composition containing anticancer medicine and its synergist The anticancer composition containing anticancer medicine and its synergist is one kind of slow releasing injection comprising slow released microsphere and solvent. The slow released microsphere includes taxane, alkylating agent and/or other anticancer medicine, rapamycin and slow releasing supplementary material. The solvent is special solvent containing suspending agent, has viscosity of 100cp-3000cp at 20-30 deg.c and is selected from sodium carboxymethyl cellulose, etc. The slow releasing supplementary material is selected from racemic lactic acid copolymer, polyethylene glycol/polylactic acid, etc. The slow released microsphere may be also prepared into slow releasing implant. The slow releasing injection and the slow releasing implant may release medicine locally for about 40 days.
US20100160400 Treatment using dantrolene Provided are low-volume, safe for injection formulations of dantrolene yielding significant advantages over the currently approved and marketed dantrolene for malignant hyperthermia (MH) threatening anesthetic crisis. Once dantrolene can be made immediately available to patients triggered of MH, the anesthesiologist will be able to focus exclusively on the management of the patient's physiologic status in this complex and evolving crisis, not on the laborious and time consuming reconstitution process of the rescue agent. The low volume, safe for injection formulations of dantrolene have significant advantages over currently used approaches to the prevention and treatment of pumphead, and other neurological, cognitive and motor dysfunction incident to iatrogenically or trauma induced situations of altered blood flow, including those incurred during surgical procedures involving CPB or related procedures, as well as those incurred during non-normothermic episodes caused iatrogenically or by disease.
CN1973839B Nizatidine injection The nizatidine injection contains nizatidine in 10-100 mg/ml, stabilizer in 5-80 vol% and at least one of pharmaceutically acceptable solubilizer and/or cosolvent in 0-5 vol%, except solvent includingwater for injection, with the stabilizer being at least one of ethanol, propylene glycol, glycerin and other lower alcohol. Test shows that the injection has high stability and safety in production and clinical application.
CN101890018A Tyrosine protein kinase inhibitor and preparation method thereof The invention relates to a tyrosine protein kinase inhibitor. The tyrosine protein kinase inhibitor is a compound represented by a general formula (1), wherein R is one or more of aryl amino, hexahydric aryl heterocycle amino, pentatomic heterocycle amino and thick heterocycle amino, which have a substituent group having the functions of coordination. The tyrosine protein kinase inhibitor has the advantages of high selectivity, fewer toxic and side effects and stronger water solubility. In addition, the tyrosine protein kinase inhibitor can be used for substituting one or more ligands in cytotoxicity organic metal ruthenium coordination compounds. The prepared coordination compound can act on protein kinase (or protein phosphatase) and can act on multiple target point-combined molecule anti-tumor compounds of DNA. The tyrosine protein kinase inhibitor is also favorable for reducing possibility that tumor cells generate medicinal resistance to medicaments.
US20080160119 Sesquiterpenoid Derivatives Having Adipocyte Differentiation Inhibitory Effect The objective of the present invention is to identify compounds having an inhibitory effect on adipocyte differentiation, and to provide pharmaceutical compositions and food compositions for prevention, improvement, or treatment of obesity or obesity related diseases. By enthusiastically studying natural products that inhibit the differentiation induction of adipocyte precursors into adipocytes, sesquiterpenoid derivatives, which are extracts from a Compositae plant, Calea, growing in Central and South America, were demonstrated to have an excellent inhibitory effect on adipocyte differentiation induction. Calea extract or the sesquiterpenoid derivatives are expected to be used in pharmaceutical compositions and food compositions for prevention, improvement, or treatment of obesity or obesity related diseases.
CN101720928A Combination for preventing and curing degenerative disease of bone and joint The invention relates to a combination for preventing and curing degenerative diseases, such as osteoporosis, osteoarthritis, and the like, comprising the following components in parts by weight: 3-30 parts of hydrolyzed collagen, 4-40 parts of glucosamine, 1.5-15 parts of calcium amino acid chelate, 0.2-20 parts of stachyose, 0.1-2 parts of vitamins C and 0.0002-0.004 parts of vitamins D3. The invention has the effects of comprehensively supplementing multiple metagenics for organisms, promoting the bone metabolism and the bone formation of human bodies, inhibiting and reducing the osteotrophy loss, inhibiting the generation and the development of the osteoporosis and the osteoarthritis, repairing the damaged articular cartilage, mitigating the pain and the moving obstacle of bone joints, reducing the incidence rate of fracture and disability, and the like and plays an active role in preventing and curing the degenerative diseases, i.e. the osteoporosis, the osteoarthritis, and the like, for the human bodies.
WO2011022596A2 Preparation of bazedoxifene and its salts Processes for preparing bazedoxifene and its pharmaceutically acceptable salts, substantially free from process related impurities and process intermediates.
WO2008070010A3 Hydroxylamine derivatives for the treatment of stroke The present invention provides methods of treating stroke comprising administering an effective amount of one or more of certain hydroxylamine derivatives to a subject in need thereof. The invention also provides pharmaceutical compositions comprising a certain hydroxylamine derivative or a pharmaceutically acceptable salt thereof, optionally in combination with one or more additional therapeutic agents. In certain compositions, the additional therapeutic agent is a second hydroxylamine derivative or a pharmaceutically acceptable salt thereof.
CN101505767A Agent for preventing infection An agent for preventing infection of influenza virus or a food and drink for preventing infection of influenza virus is provided. The agent for preventing infection of influenza virus and food and drink for preventing infection of influenza virus containing a fat globule membrane component as an active ingredient. The agent for preventing infection of influenza virus and food and drink for preventing infection of influenza virus containing a phospholipid with sphingosine and/or a derivative thereof, particularly sphingomyelin as an active ingredient.
WO2011117254A1 Piperidine amides as modulators of the ghrelin receptor Compounds of formula (I) or pharmaceutically acceptable salts thereof, are useful for the treatment of diabetes and obesity.
US20100272680 Piperidinyl Cyclic Amido Antiviral Agents Provided are compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).
US20090018159 Treatment of Diabetes The invention relates to the use of a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety, or a tautomer, a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof for the manufacture of a medicament for the treatment of diabetic patients.
WO2007146039A2 Crystalline forms of n-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl] thio]-2-thiazolyl]-4-piperidinecarboxamide Crystalline forms of N-[5-[[[5-(l,1 -dimethylethyl)-2-oxazolyl]methyl]thio]-2- thiazolyl]-4-piperidinecarboxamide are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of N-[5-[[[5-(l,l-dimethylethyl)- 2-oxazolyl]metliyl]thio]-2-thiazolyl]-4-piperidinecarboxamide, as well as a method of using one or more crystalline forms of N-[5-[[[5-(l,l-dimethylethyl)-2- oxazolyl]methyj]thio]-2-thiazolyl]-4-piperidinecarboxarnide in the treatment of cancer and other proliferative diseases.
WO2012107364A1 Novel composition for the treatment of cystic fibrosis The present invention provides a composition comprising at least one prostacyclin orprostacyclin analogue or a pharmaceutically acceptable salt thereof and at least one compound selected from the group consisting of leukotriene antagonists, prostaglandin antagonists and duramycin or a pharmaceutically acceptable salt thereof for use in preventing or treating cystic fibrosis. The invention also provides a composition comprising Treprostiniland a compound from the group consisting of leukotriene antagonists, prostaglandin antagonists and duramycinor a pharmaceutically acceptable salt thereof.
CN1872107B Chinese and Western compound preparations of alpha receptor blocking pharmacon, preparation method, and application A compound medicine able to block the alpha receptor for treating periperal vascular spasm, infectious shock, pheochromocytoma, prostatoplasia, ED and prospermia is prepared from phenoxybenzamine hydrochloride, the extract of largespike woodnettle root and auxiliary.
CN103304564A Beta-carboline derivative containing hydroximic acid as well as preparation method and medical application thereof The invention discloses a beta-carboline derivative containing hydroximic acid as well as a preparation method and a medical application thereof. The product has the structure as shown in the general formula I. The compound can be combined with other antitumor drugs such as alkylating agents, antimetabolites, topoisomerase inhibitors, mitotic inhibitors and DNA intercalating agents and additionally can be combined with radiotherapy. The invention also discloses a pharmaceutical composition containing the compound with the general formula I as well as medical application thereof, particularly application of preparation of antitumor medicines, Alzheimer disease medicines and Parkinson disease medicines. The other antitumor medicines or radiotherapy can be administrated with the compound at the same time or in different times. The combination therapy can generate the synergistic effect, so that the treatment effect is improved.
EP1587801B1 A process for preparing duloxetine and intermediates for use therein A process for preparing (+)duloxetine, or an acid addition salt thereof, which process comprises resolving racemic (±)duloxetine with a chiral acid so as to obtain a salt of the chiral acid and (+)duloxetine, substantially free of (-)duloxetine; and (ii) if desired, converting the salt prepared in step (i) to the free base or another acid addition salt as appropriate. The process for preparing (+)duloxetine, or an acid addition salt thereof, can further comprise an O-alkylation intermediate process step which is carried out in the presence of a base and a phase transfer catalyst.
EP1840123A1 Isoxazolines and their use as inhibitors of phosphodiesterase type-IV The present invention relates to isoxazoline derivatives of formula I, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.
CA2163363C Stable suppository formulations effecting biovailability of .delta.9-thc Suppository formulations having long-term stability and containing readily bioavailable .DELTA.9-THC derivatives.
CN102688186A Medicine composition containing vinpocetine raw material The invention belongs to the technical field of medicines, and provides a medicine composition containing vinpocetine raw material. The medicine composition comprises vinpocetine raw material, sodium chloride and cosolvent, and is prepared into aqueous solution. Research indicates that: the vinpocetine raw material and cosolvent have higher stability at a certain weight proportion; and further research shows that: the quality of the vinpocetine raw material has certain impact on the stability. The stability test shows that: the preparation prepared from the composition provided by the invention has higher stability.
WO2005067942A1 Glycosaminoglycan peptides derived from connective tissues and use thereof in the prevention of arthritis and other degenerative medical conditions The inventors sought to provide compositions and methods of prophylaxis to prevent these harmful immune responses in patients and to prevent the related undesirable symptoms biological tissue such as for example inflammation, cell injury, tissue injury, tissue degradation, tenderness, redness, joint stiffness, joint swelling, restricted mobility and reduced strength. The inventors found that prophylactic therapy of an animal comprising administering a pharmaceutical composition comprising a GAG-peptide complex, optionally together with a connective tissue derived polypeptide, prevented the onset of at least one undesirable symptom.
USRE40089 Nucleic acid molecules encoding the MAGE-1 tumor rejection antigen precursor The invention relates to an isolated DNA sequence which codes for an antigen expressed by tumor cells which is recognized by cytotoxic T cells, leading to lysis of the tumor which expresses it. Also described are cells transfected by the DNA sequence, and various therapeutic and diagnostic uses arising out of the properties of the DNA and the antigen for which it codes.
CN102070429A Chalcone derivative, and preparing method and application thereof The invention discloses a chalcone derivative, and a preparing method and application thereof, which relate to chalcone and provide the chalcone derivative. The chalcone derivative is yellow oily liquid, the chemical name is 3,3'-diallyl-4,4'-dihydroxy chalcone, and the molecular weight is 320.1. Claisen rearrangement reaction is utilized, the chalcone derivative can be conveniently and fast prepared, the preparing method is simple, used raw materials have a low price, and the preparing method can be widely applied to industrialized production. The 3,3'-diallyl-4,4'-dihydroxy chalcone has thesimilar structural characteristics to 4,4'-dihydroxy chalcone, and the antineoplastic activity of the 3,3'-diallyl-4,4'-dihydroxy chalcone is obviously improved through being compared with that of the 4,4'-dihydroxy chalcone. The growth of tumour cells can be obviously inhibited, and the chalcone derivative has wide application to antineoplastic medicine preparation.
US20110200564 Diagnosis and treatment of alzheimer's disease (ad) Disclosed herein are novel methods, assays and systems for detecting an increased risk for Alzheimer's disease (AD) in a subject by identifying at least one nuclei acid polymorphism described herein in a biological sample from the subject. Levels of the genes associated with the nucleic acid polymorphism described herein are also determined for detection of higher risk for AD. Disclosed herein further provides methods for treating AD by administering to a subject in need thereof with ATXN1.
US20120009273 Kit of pharmaceutical formulations characterized by the presence of molecular oxygen An array of pharmaceutical formulations characterized by the presence of molecular oxygen comprising four elements which, in combination, furnish benefits for the health of patients with HIV AIDS: (i) weight increase of the patient; (ii) increase of appetite; (iii) reduction of diarrhea; (iv) reduction of the wasting syndrome; (v) increase of stability of mood; (vi) increase of muscular mass. (vii) decrease of opportunistic diseases, in particular infections caused by Candida, herpes virus, cytomegalovirus, Kaposi's sarcoma; (viii) prolongation of the period wherein the patient does not require to take antiretrovirals; (ix) increase of acceptance of pharmacological treatment; x. reduction of gastritis, nausea or vomiting, headache; (xi) reduction of cases with anemia or thrombocytopenia; and (xii) a change in the phase of the disease in the patient.
US7741328 Treating inflammatory diseases such as rheumatoid arthritis, multiple sclerosis or Crohn's disease; Very Late Antigen-4 (VLA-4), also called alpha 4 beta 1 integrin; N-(sulfonamido-substituted pyrimidyl, pyridyl or pyrazyl)-L-4-(N,N-dimethylcarbamyloxy)phenylalanine compounds Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
CN103169650A Anti-flu syrup and preparation method thereof The invention discloses an antivirus medicine, and in particular relates to anti-flu rimantadine hydrochloride syrup and a preparation method thereof. The anti-flu syrup is prepared from raw materials in parts by weight as follows: 5-7 parts of rimantadine hydrochloride, 1-1.5 parts of citric acid, 0.1-0.15 parts of strawberry essence, 0.1-0.5 parts of sodium benzoate, 300-400 parts of cane sugar and 600 parts of purified water. The anti-flu syrup provided by the invention has the advantages that the syrup is easier to absorb by human body, and the curative effect is more remarkable; and the syrup has the characteristics of low cost, small amount of auxiliary materials, high bioavailability, good medical effect and good compliance. The preparation method of the anti-flu syrup provided by the invention has the characteristic of simpleness and easiness in control of the preparation process, and the production cost is lowered while the medicine quality is ensured.
CN1795925A Medication composition of plant estrogens for treating colpitis A composite vegetative estrin medicine in the form of suppository, gel or film for treating vagititis and improving the toughness of vagina and its resistance to bacteria is proportionally prepared from vegetative estrin, cnidiadin, borneol, and at least one of matrine, phellodendrine, berberine, etc and their physiocologically acceptable salts.
WO2012156317A2 Intranasal pharmaceutical dosage forms comprising naloxone The present invention relates to an intranasal pharmaceutical dosage form comprising a dosing unit comprising naloxone or a pharmaceutically acceptable salt thereof in an amount of equivalent to ≥ 0.5 mg naloxone HCl dissolved in an application fluid of a volume of ≤ 250 µl. Furthermore, the present invention relates to such an intranasal pharmaceutical dosage form for use in the treatment of opioid overdosing and/or at least one symptom thereof.
WO2007010504A2 Acid addition salts of isoindoles acting as adrenergic receptor antagonists Provided herein are acid addition salts of compounds of Formula (I). The acid addition salts of Formula I described herein can be used to treat benign prostatic hyperplasia (BPH) and the related symptoms thereof. Further, these compounds can be used to treat lower urinary tract symptoms (LUTS) that may or may not be associated with BPH. Process for preparing the compounds described herein, pharmaceutical compositions thereof, and the methods of treating BPH or related symptoms thereof and LUTS that may or may not be associated with BPH are also provided.
EP1259261B1 Pharmaceutical compositions comprising terbinafine Pharmaceutical compositions for oral administration comprising terbinafine, a buffering component and a disintegrant. The compositions show rapid disintegration and having taste-masking properties.
US20130237511 Copper Ion Delivery Platform for Pharmaceutical Agents Methods for utilizing copper ions to bind to and help transport medicinal agents that contain a nitrogen atom or atoms are disclosed. The copper ion or ions serve as a delivery platform for a known pharmaceutical agent. The copper ions may be used to impact the polarity of the medicinal agents so they perform more efficiently in a physiological environment. The copper ions may also improve the efficacy of the drug by impacting their stability.
US7973040 Macrocyclic quinoxaline compounds as HCV NS3 protease inhibitors The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections.
US20100166739 Methods and Compositions for Diagnosing Urological Disorders It has been discovered that cytokines, chemokines, and growth factors in urine are biomarkers indicative of urological disorders including interstitial cystitis/painful bladder syndrome and overactive bladder syndrome. Preferred chemokine biomarkers are CCL2, CCL4 (MIP-1β), CCL11, CXCL1 (GRO-α), sCD40L, IL-12p70/p40, IL-5, sIL-2Rα, IL-6, IL-10, IL-8, and EGF. The concentration of one or more of these chemokines in an urine sample can be used to assist in the diagnosis of urological disorders. Methods for evaluating the effectiveness of treatments for urological disorders and for assessing the severity of urological disorders are also provided.
CN103040094A Gardenia fragrance type snuffs The invention belongs to the technical field of snuff productions and relates to gardenia fragrance type snuffs and a preparation method thereof. The gardenia fragrance type snuffs are composed of the following natural raw materials of 100-500 parts of green tea, 0.05-0.35 part of musk, 50-150 parts of fructus amoni, 10-90 parts of poria, 100-300 parts of mint leaf, 0.1-0.4 part of borneol, 0.03-0.10 part of assrum, 0.01-0.09 part of rhino horn, 5-15 parts of rhizome acori graminel, 25-125 parts of tobacco, 2-6 parts of elecampane, 2-6 parts of flos caryophylli, 5-25 parts of radix angelicae, 2-6 parts of menthol and 50-150 parts of red wine. The gardenia fragrance type snuff is fumigated by gardenia and has a delicate fragrance of gardenia. The gardenia fragrance type snuffs have the advantages of being capable of refreshing, enabling the nasal cavity to breath and helping giving up smoking.
US20110136786 Method of treating mood disorders Methods of treating mood disorders comprising administering an effective amount of 11-piperazin-1-yldibenzo[b,f][1,4]thiazepine or a pharmaceutically acceptable salt thereof and pharmaceutical compositions therefor.
CN101530494A Substance for intestinal tract lavation and toxin expelling and preparation method thereof Substance for intestinal tract lavation and toxin expelling and a preparation method thereof are used for human intestinal tract toxin expelling. The substance for intestinal tract lavation and toxin expelling comprises stachyose, coffee bean, lactobacillus fermentation liquid, inorganic salt extract, natural lemon freeze drying powder and pure water. The substance for intestinal tract lavation and toxin expelling can adjust acid-base balance, flora balance and electrolyte balance in intestinal tract, a preparing and using method for intestinal tract lavation and toxin expelling can reinforce liver metabolism, promote bile secrete, protect liver, remove blood toxin, adjust intestinal tract of human to ideal state, make function of the intestinal tract more health and the metabolic of the intestinal tract more smooth, so that the intestinal tract has no dependence.
US6958218 Detecting modulators of brain membrane protein; obtain membrane protein, incubate with ligand and labeled compound, measure level of binding A method for the screening of ligands which bind to soluble α2δ-1 subtype polypeptides.
CN103169713A Anticancer application of sterols derivative The invention belongs to the field of medicine and chemical industry, and relates to an anticancer application of a sterols derivative. The sterols derivative is a compound shown as the formula I, or a pharmaceutically acceptable salt thereof, wherein R1 is selected form -OH, =O, H and C1-C3 alkyl; R2 is selected form -OH, H and C1-C3 alkyl; R3 is selected form -OH, =O, H and C1-C3 alkyl; R4 is selected form -OH, H and C1-C3 alkyl; and any two, three or four of R1, R2, R3 and R4 are -OH simultaneously. The compound provided by the invention is capable of effectively inhibiting proliferation of cancer cells (tumor cells), and the inhibition effect is in concentration-effect relationships, thus the sterols derivative has the potential of a medicament for prevention and/or treatment and/or adjuvant treatment of cancers.
CN102499927A Medicine composition for preventing and curing tumors The invention relates to medicine composition for preventing and curing tumors, which effectively prevents and cures the tumors. The technical scheme includes that the medicine composition is prepared, by mole ratio, by from 1 to 20 parts of 2- methoxyestradiol and from 1 to 40 parts of curcumin derivant in a mixing manner, and the curcumin derivant is mixture of more than one or two of curcumin, demethoxycurcumin and bisdethoxy curcumin which have equal mole ratios; and the medicine composition is prepared into one of tablets, capsules, dripping pills, micro pills, oral liquid, freeze-drying preparation, injection, infusion solution, suppository, ointments, babu plaster and transdermal agent. The medicine composition is low in cost, has multi-target and multipurpose anti-tumor effects, is safe and reliable, effectively improves treatment compliances of patients, and plays an important role in preventing and curing the tumors to the greatest extent.
CN102245184A Enzastaurin for the treatment of cancer The present invention relates to HDAC2 as a biological marker for treating cancer in a patient using Enzastaurin as a single agent or in combination with a Class I selective HDAC inhibitor.
US20120027818 Bisphosphonate product in a cycloolefinic polymer container A pharmaceutical product comprises a container containing a bisphosphonate solution, in which at least the internal surface of the container comprises a plastic material and in which the container is heat sterilisable, and which is in the form of an infusion solution preconcentrate for administration of the bisphosphonate to a patient in need of bisphosphonate treatment.
CN1968949A Proline derivatives and their use as dipeptidyl peptidase IV inhibitors The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R<1>, R<2>, R<3>, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.
US20090035256 Modified interleukin 10 polypeptide for use in treatment and prevention of neuropathic pain, neurological and inflammatory disorders IL-10 sequence variants are disclosed that retain the therapeutically desirable anti-inflammatory properties of wild-type IL-10 but do not retain the hemoatopoeitic cell regulatory and cell proliferative activities. The mutant IL-10 polypeptides of the invention are used in methods of treating diseases involving inflammatory response, including neuropathic pain and other neurological disorders.
WO2009001805A1 Novel artificial n-linked sialo-sugar chain-containing polymer and method for producing the same It is intended to provide a sialo-sugar chain-containing polymer, which can be synthesized by a practical method capable of achieving a high synthetic yield and has an improved infection inhibitory activity against an influenza virus, and a method for producing the same. An N-linked sialo-sugar chain-containing polymer which is represented by the following structural formula (I) and in which a sialo-sugar chain has been linked to γ-polyglutamic acid via a compound having an amino group and a carboxyl group at an end thereof as a linker. Formula (I) (In the formula, Z means a hydroxy group or a residue represented by the formula (II), and n represents an integer of 10 or more, with the proviso that any one or more of the Z's is a residue represented by the formula (II).) Formula (II) (In the formula, X means a hydroxy group or an acetylamino group, Y1 and Y2 means a hydroxy group or an N-acetylneuraminic acid residue, L means a hydrocarbon, and m represents 0 or an integer of 1 or 2, with the proviso that Y1 and Y2 are not the same.)
US20130059885 Method For Preparation Of Pitavastatin and Pharmaceutical Acceptable Salts Thereof The present invention discloses a compound, which is alkali or alkaline earth metal salts of pitavastatin, wherein the alkali or earth metal comprise one or more of magnesium, zinc, potassium, strontium and barium.
EP2039681A1 Cycloalkene derivatives, process for production of the derivatives, and use of the same The present invention relates to a cycloalkene derivative represented by the formula (I): wherein each symbol is as defined in the specification, a pharmaceutical agent containing the derivative, and a production method thereof. The cycloalkene derivative of the present invention has high solubility in water and is suitable for use as an injection.
CN103142562A Sustained-release sticking film for treating oral ulcer The invention discloses a sustained-release sticking film for treating oral ulcer and relates to the technical field of medical equipment and preparation technology thereof. The sustained-release sticking film is of a circular sheet and provided with a three-layer structure, wherein the upper layer is a sustained-release coating (1) which contacts with an oral ulcer surface, the lower layer is a polyacrylic acid film (3) with a protective effect, a medicament-loaded layer of the middle layer takes bacterial cellulose as a medicament carrier, and a medicament loading substance with a sustained-release effect enters a bacterial cellulose membrane by using a dipping method to obtain a bacterial cellulose/medicament loading substance composite film (2). The sustained-release sticking film disclosed by the invention is good in adhesion, permeability and biocompatibility, large in medicament loading capacity, long in local effect time, capable of relieving pain, promoting wound healing and preventing wound infection. The sustained-release sticking film is suitable for oral traumas of oral ulcers, oral mucosal bites and the like.
EP2229162A2 Substituted benzoquinones and hydroquinones in the treatment of periodontal diseases An alkyl- or halo-substituted benzoquinone, hydroquinone or mixture thereof, for use in the treatment of a periodontal disease, and/or for use in the treatment of a condition which is caused by, transmitted by or exacerbated by P. gingivalis or by biofilm formation by P. gingivalis.
CN103202815A Injection for treating mental disease The invention relates to an injection for treating mental disease, and particularly relates to a freeze drying power-injection. The freeze drying power-injection contains a compound serving as an active ingredient and shown in the formula I shown in the description or pharmaceutically acceptable salts of the compound, mannitol and/or glycine serving as excipient and an optional pH conditioning agent, wherein the weight ratio of the excipient to the active ingredient is (1-1000): 1. The freeze drying power-injection has good stability.
EP2723732A1 Trpv1 antagonists including dihydroxy substituent and uses thereof The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R1, R4, R8, R9, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.
CA2413883C Method for preventing tissue damage associated with graft-versus-host or host-versus-graft disease following transplantation A method for preventing tissue damage associated with graft-versus-host disease in a patient having undergone hematopoietic cell transplantation, and host-versus-graft disease in a patient having undergone organ allograft transplantation. The method includes orally administering to the patient a prophylactically effective amount of a topically active corticosteroid, such as beclomethasone dipropionate, for a period of time following hematopoietic cell or organ allograft transplantation, and prior to the presentation of symptoms associated with graft-versus-host disease or host-versus-graft disease. Representative tissues includes tissue of the intestine and liver, while representative tissue damage includes inflammation thereof.
US20120004248 Methods of using a methylxanthine compound The invention relates to compositions and methods for treating various diseases or medical conditions by administering a methylxanthine compound. Specifically, the invention relates to compositions and methods for treating cytochrome oxidase (CcOX) mediated diseases or medical conditions by administering compositions comprising a methyl xanthine compound.
CN102108090A Dihydroiso-coumarin glucoside compounds and preparation method and application thereof The invention discloses new dihydroiso-coumarin glucoside compounds shown in a formula I, which are extracted and separated from Periplaneta americanna medicinal materials. Through mouse auricle swelling tests, rat granulation tissue hyperblastosis tests and the like, results show that the compounds have effects of resisting inflammation, promoting wounds to heal and the like; and the compounds can be used for preparing medicines for treating inflammation, ulcers, wounds, incised wounds, fistula, burn, scalding and the like, particularly medicines for preventing and treating diseases related to inflammation resistance, promotion of granulation tissue hyperblastosis, wound healing and the like, and have high clinical application value. The invention provides a preparation method for the compounds shown in the formula I.
US7846679 Methods for detecting the presence of mutant mammalian presenilin protein The present invention describes the identification, isolation, cloning, and determination of the Alzheimer Related Membrane Protein (ARMP) gene on chromosome 14 and a related gene, E5-1, on chromosome 1. Normal and mutant copies of both genes are presented. Transcripts and products of these genes are useful in detecting and diagnosing Alzheimer's disease, developing therapeutics for treatment of Alzheimer's disease, as well as the isolation and manufacture of the protein and the construction of transgenic animals expressing the mutant genes.
US20120071506 Methods for treating cns disorders with bicyclo-substituted 2-imidazoline and 2-imidazoles The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification, and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms. The invention also relates to novel compounds of formula I, compositions containing them, and methods for their preparation.
US20080051373 Parenteral preparations of GI-safer phospholipid-associated anti-inflammatories and methods of preparation and use Parenteral preparations of phospholipid-associated anti-inflammatories (PL-AIs) are described to treat pain/inflammation, with reduced gastrointestinal (GI) toxicity. The PL-AIs can be composed of phosphatidylcholine (“PC”) associated with non-steroidal anti-inflammatory drugs (“NSAIDs”). To prepare the PL-AIs, a phospholipid is mixed with an NSAID in a polar solvent, solvent is removed, suspended in an aqueous medium and sterilized by filtration or other acceptable method. Alternatively, the phospholipid can be mixed with an injectable preparation of an NSAID. The PL-AIs, and particularly PC associated with the NSAIDs, indomethacin, ibuprofen or diclofenac are useful for treating Patent Ductus Arteriosus in low birth weight infants to reduce the incidence of GI injury that may be manifest as Necrotizing Enterocolitis (NEC) or Spontaneous Intestinal Perforation (SIP). Other applications of the parenteral PL-AIs include prevention of: retinopathy of prematurity; and of pain from conditions associated with surgery, trauma, Sickle Cell Anemia and neural inflammation/injury.
WO2008135793A1 Combination of aplidine and carboplatin in anticancer treatments Methods for treating a human patient afflicted with cancer, comprising administering to said patient a therapeutically effective amount of Aplidine in combination with Carboplatin are provided.
US20120189607 Method of regulating fertilizing ability using cyclic adp-ribose and cd38 The present invention relates to a pharmaceutical composition for promoting fertilization comprising cyclic ADP-ribose or its derivative, CD38 and to a method of promoting fertilization by promoting the synthesis of cyclic ADP-ribose to increase sperm motility. Also, the present invention relates to a pharmaceutical composition for contraception and a method for inhibiting fertilization, which can inhibit the expression or function of cyclic ADP-ribose to reduce sperm motility, thereby inhibiting fertilization.
WO2011113300A1 Medicines for inhibiting toxicity or side effects caused by chemotherapeutic agents Compounds of formula (1) or a derivative thereof, acipimox, are used in combination with several chemotherapeutic agents for inhibition of toxicity or side effects caused by chemotherapeutic agents, while do not attenuate chemotherapeutic effects, wherein n represents Arabic numbers, X represents O or NR3, R1 represents H, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cyclic ether group, which are optionally substituted by one or more groups selected from hydroxyl, carboxyl, amino group, C1-C6 alkyl or C1-C6 alkoxyl, R2 represents H, halogen, carboxyl, nitro, amino group, hydroxyl, C1-C6 alkyl or C1-C6 alkoxyl, R3 represents H or C1-C6 alkyl.
CN102247436A Preparation method of Qingxuanpian The invention discloses a preparation method of Qingxuanpian. The technology of integrating diaphragm filter pressing, circulating, extracting and separating is used for replacing the existing boiling method and reflux method to extract effective ingredients of prescription drug. Thus, the technical flows are greatly simplified, a production period is greatly shortened, energy consumption is saved, and the preparation method is favorable for environmental protection and waste residue utilization. In addition, the use amount of ethanol which is extraction solvent can be greatly reduced, and the recovery rate of the effective ingredients can be greatly improved.
US6984632 Complexes of paroxetine, with cyclodextrins or cyclodextrin derivatives Complexes of paroxetine, as free base or salt, with a cyclodextrin or a cyclodextrin derivative having a molar ratio between paroxetine and cyclodextrin ranging from 1:0.25 to 1:20, suitable for use in liquid and solid pharmaceutical compositions for oral and parenteral administration.
US7030104 Topical oestroprogestational compositions with a systemic effect The present invention relates to the field of therapeutic chemistry and more especially to the realization of new galenic forms intended to be applied on the skin. More particularly it relates to a topical hormonal composition with a systemic effect for the hormonal treatment of the perimenopause and of the menopause as well as for the treatment of the ovarian hormonal deficiencies in women with amenorrhea, characterized in that it comprises, as active ingredients, a progestogen derived from 19-nor progesterone and estradiol or one of its derivatives, a vehicle which allows the systemic passage of said active ingredients, chosen from the group constituted by a solubilizing agent, an absorption promoting agent, a film-forming agent, a gelling agent and their mixtures, in combination or in a mixture with suitable excipients for the realization of a gelled and/or film-forming pharmaceutical form.
US20120136061 Lycopene and resveratrol compositions for nk cell activation resulting in anti-neoplastic effect A carotenoid and a terpenoid in therapeutically-effective amounts is disclosed such that, upon ingestion in one preparation, or in two separated preparations, simultaneous or sequentially, and upon metabolism, the activity of natural killer (NK) cells is elevated. Specifically, the composition comprises lycopene and resveratrol in the range of 1:10 to 10:1 by molar; more preferably 1:1 to 3:1 by molar, and most preferably at 3:1. Alternatively, the preferred ratio may be expressed as 1:4 to 25:1 by weight; more preferably 2½:1 to 7½:1 by weight, and most preferably at 7½:1. The composition may be formulated for oral intake as a pharmaceutical, dietary supplement or food product and provided in therapeutically effective amounts to a mammal, preferably in a dosage of about 3.5 mg per day per 20 g of a mammalian body mass in a ratio of 2½:1 by weight, which can be translated to about 400 mg to 1000 mg per day for a typical human in need of elevating NK cell activity. Preferably, the therapeutically-effective aspect of the composition includes its metabolically-producing agents, prodrugs, metabolites or intermediate compounds useful in triggering NK cells into cytotoxic or cytolytic response.
CN102525971A Gastrointestinal motility promoting medicinal oral disintegrating tablets and preparation method thereof The invention discloses gastrointestinal motility promoting medicinal oral disintegrating tablets and a preparation method thereof, and relates to gastrointestinal motility promoting medicinal oral disintegrating tablets and a formulation and a technology for preparing the gastrointestinal motility promoting medicinal oral disintegrating tablets by adopting a freeze drying method. The gastrointestinal motility promoting medicinal oral disintegrating tablets are prepared from main medicaments and medicinal auxiliary materials, have good mouthfeel, do not have grit feeling, and greatly improve the medication compliance of patients; the tablets do not require water during administration, can be quickly disintegrated after the tablets enter the mouth, do not cause vomiting reflex, and provide great convenience for the patients; the tablets are suitable to be taken in journey under the condition that a water source is not easily obtained; the tablets have the advantages of convenience in administration, quick absorption, low first pass effect, low irritation to digestive tract mucosa and the like, and have a broad market application prospect; and the gastrointestinal motility promoting medicinal oral disintegrating tablets can obviously reduce the side effects of a gastrointestinal motility promoting medicament. In addition, the invention also relates to the preparation method for the gastrointestinal motility promoting medicinal oral disintegrating tablets.
CN101670052A Drug for treating Meniere disease and preparation method thereof The invention relates to a drug for treating Meniere disease, which is a capsule product prepared by the following steps of evenly mixing purified pinellia tuber, stir-fried liquoric root, red ochre and magnetite with membranous milkvetch root, inula flower, tangerine peel, bitter orange, bamboo shavings, Indian buead, chrysanthemum, barbary wolfberry fruit, kudzuvine root and oriental waterplantain rhizome, adding water for decoction, then concentrating into a thick paste, drying, smashing, packaging into capsules and carrying out sterilization and disinfection. The drug has the effects of benefiting qi, regulating stomach, dissipating phlegm, lowering adverse qi, suppressing hyperactive liver and calming wind and is characterized by actual efficacy, rapidness, convenience and safe administration for treating the Meniere disease. The clinical observation shows that the effective rate of the drug is 96.0%.
US20090274677 Antioxidant for use in cosmetic, medicated and pharmaceutical preparations The invention provides the use a 2,2-dimethyl chroman as a SOD mimetic in a cosmetic preparation. Cosmetic preparations comprising a 2,2-dimethyl chroman as a SOD mimetic are described, as well as methods for treating or preventing free radical damage to skin cells and treating or preventing hair loss which comprise topical administration of a 2,2-dimethyl chroman as a SOD mimetic.
US20080057136 An ionogenic surfactant, a metal chelating complex with an affinity for protons, solvent and carrier; preferably cetylpyridinium chloride, EDTA-zinc complex, and isopropanol; fungicides for oral, topical or intravenous administration; dandruff, acne, dermatitis The invention relates to antimicrobial compositions that can be used for disinfecting and can be applied in various aspects of the national economy, medicine, and laboratories of all types. The antimicrobial compositions comprise a chelating metal complex compound with a monodentate bidentate or polydentate ligand that exhibits affinity to hydrogen ion, an ionogenic surfactant, and a solvent. The compositions of the invention display antiseptic properties. The antimicrobial compositions are active against Gram-positive and Gram-negative bacteria, fungi, viruses, and spores, and can be applied in a broad temperature interval. Methods of using the compositions of the present invention in the treatment and prevention of diseases caused by a variety of pathogens are further provided.
CN102716321A Method for processing neurosis capsules The invention relates to a method for processing neurosis capsules having a formula of medical materials comprising pilose asiabell root, feihuoshi, chrysanthemum, etc. By using a dreg-removing and concentrating manufacture method, radix rehmanniae and aged wine, in a ratio of 1:2.5 by kilogram, are boiled together with a small amount of vinegar, and then dregs are removed and juice is taken to reserve. Medical materials of plantain, Sichuan-produced coptis and honeysuckle are boiled in water after being smashed, and then dregs are removed and juice is taken to reserve. Medical materials of monochoria vaginalis, chrysanthemum and cortex moutan are soaked in water for half an hour, and then boiled and juice is taken to reserve. The three kinds of reserved juice are mixed and then together with unused medical materials in the formula, are stirred, dried in the sun and grinded in all to obtain powder. The powder is sifted over a 180 mesh sieve and then made into capsules. Four to five capsules can be taken at every time, twice per day, and a treatment course is 100 days. When the capsules are taken for a month, symptoms of insomnia, red leucorrhoea, cystitis, etc., are improved obviously. When the capsules are taken throughout the treatment course, neurosis and anemia can be treated forever and a plurality of gynecologic diseases can be recuperated at the same time. Effects of skin whitening, beauty improving, and skin softening can be also achieved.
CN102716128A Pharmaceutical composition for treating asthma The invention discloses a pharmaceutical composition taking ambroxol hydrochloride and montelukast sodium as active ingredients and the application of the pharmaceutical composition. The composition can be made into oral preparations including tablets, capsules, granules, chewable tablets, oral solutions and dry suspensions. As the ambroxol hydrochloride and the montelukast sodium are synergistic, the composition has an unexpected effect of treating asthma and is very good in application prospect.
CN103719437A Bulbus fritillariae cirrhosae health care tea for treatment of hemorrhoid The invention relates to bulbus fritillariae cirrhosae health care tea for treatment of hemorrhoid, the bulbus fritillariae cirrhosae health care tea for treatment of the hemorrhoid is prepared as follows: proportionally mixing 26 parts of bulbus fritillariae cirrhosae, 13 parts of golden cypress, 11 parts of borneol, 14 parts of radix sophorae flavescentis, 13 parts of pericarpium citri reticulatae and 23 parts of catechu of a herbal tea formula, finely selecting, cleaning, drying and crushing, detecting the quality, weighing, filling in a non-woven inner bag, and hot pressing for sealing, and the bulbus fritillariae cirrhosae health care tea for treatment of the hemorrhoid is simple in production method, easy to carry and brew, has the efficacy of relieving swelling, stopping pain, clearing heat and detoxication, can help people to clear heat, promote dieresis, and alleviate hemorrhoids by long term drinking.
CN1857271A Black/white preparation recipe for treating psychosis The present invention relates to a kind of psychosis treating black/white medicine preparation. The psychosis treating black/white medicine preparation includes one black preparation for night taking and one white preparation for day time taking, and each of the black preparation and the white preparation consists of antipsychotic components and clonazepam. The black preparation with the functions of treating psychosis, dissipating anxiety, tranquilizing and promoting sleep, and the white preparation with the functions of treating psychosis, dissipating anxiety and treating depression cooperate to reach raised psychosis treating effect.
EP2204368A1 4-sulfonylpiperidine derivatives [PROBLEMS] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [MEANS FOR SOLVING PROBLEMS] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms -CH2-CH2- or the like, or M4 together with M2 or M3 forms -CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one -CH2- or - CH2-CH2- group is formed thereamong.
EP1854509A2 Methods and compositions for restoring conformational stability of a protein of the p53 family There is provided the use of an organic non-peptide compound that binds to one or more domains of a human protein of the p53 family under physiological conditions and stabilizes a functional conformation therein for the preparation of a medicament for promoting the activity of a human protein of the p53 family, wherein one or more functional activities of said protein are at least partially impaired by the inability of said protein to maintain a functional conformation under physiological condition. Such compound may be used in the treatment of cancer due to impaired activity of p53 family proteins (p53,p63 or p73).
WO2009086720A1 2,3,4,6-tetra-o-acetyl-d-glucopyranosyl-[n,n'-di-(2-chloroethyl)]-phosphoric acid diamide, preparation methods and uses thereof 2,3,4,6-tetra-O-acetyl-D-glucopyranosyl-[N,N'-di-(2-chloroethyl)]-phosphoric acid diamide I, its α-configuration II and its β-configuration III. These compounds show inhibitory action on transplantation tumors in mouse from the pharmacodynamic test and low toxicity from pharmacological toxicity test. So these compounds can be used for preparation of anti-tumors drugs. The preparation methods of compounds I,II,III are brief reaction steps, high yields, low cost and suitable for industrialization.
US20120065205 Pyrazine carboxamide orexin receptor antagonists The present invention is directed to pyrazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
US6924300 Oxyiminoalkanoic acid derivatives To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance. A compound represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond, —CO—, —CH(OH)— or a group represented by —NR6— wherein R6 is a hydrogen atom or an optionally substituted alkyl group; n is an integer of 1 to 3; Y is an oxygen atom, a sulfur atom, —SO—, —SO2— or a group represented by —NR7— wherein R7 is a hydrogen atom or an optionally alkyl group; ring A is a benzene ring optionally having additional one to three substituents; p is an integer of 1 to 8; R2 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; q is an integer of 0 to 6; m is 0 or 1; R3 is a hydroxy group, OR8 (R8 is an optionally substituted hydrocarbon group.) or NR9R10 (R9 and R10 are the same or different groups which are selected from a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group or R9 and R10 combine together to form a ring); R4 and R5 are the same or different groups which are selected from a hydrogen atom or an optionally substituted hydrocarbon group wherein R4 may form a ring with R2; provided that when R1 is a ethoxymethyl, a C1-3 alkyl, phenyl or p-methoxyphenyl and q=m=0, R3 is NR9R10; and provided that O-[2-chloro-4-(2-quinolylmethoxy)phenylmethyl]oxime and a methyl pyruvate of [2-chloro-4-(2-quinolylmethoxy)phenylmethyl]-2-iminoxypropionic acid are excluded; or a salt thereof.
US7329649 Combinatorial methods for inducing cancer cell death The present invention relates to methods and compositions for inhibiting proliferation and inducing cell death in a population of cancer cells by (i) increasing the amount of the differentiation associated protein MDA-7, and (ii) decreasing RAS activity within the population. It is based, at least in part, on the discovery that decreasing expression of a mutated, activated K-ras gene, together with introducing an expressible mda-7 gene, in pancreatic cells had a synergistic growth-inhibitory and anti-survival effect, and abolished tumorigenicity of the cells in athymic nude mice. The methods of the invention may be directed to the therapy of pancreatic cancer and other malignancies.
WO2013001412A1 Compositions for the treatment of fragile x syndrome The present invention relates to a composition comprising a maxi-K potassium channel opener the use in the treatment of fragile X syndrome. More specifically the present invention relates to a composition comprising a fluoro- oxindole or a chloro-oxindole for use in the treatment of fragile X syndrome.
WO2010026238A1 Combination preparation for treating cancer The present invention relates to pharmaceutical compositions for treating cancer illnesses, comprising at least one statin or a pharmaceutically suitable salt or solvate thereof, and comprising the active ingredient Astemizol or a pharmaceutically suitable salt or solvate thereof. In particular, the invention relates to a pharmaceutical composition comprising the statin Atorvastatin and/or the statin Lovastatin and the active ingredient Astemizol or pharmaceutically suitable salts or solvates of said compounds. The invention further provides kits comprising said compounds.
CA2713997A1 New 2,3,4,5-tetrahydro-1h-pyrido[4,3-b]indole compounds and methods of use thereof This disclosure relates to new tricyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds are described, including new 2,3,4,5- tetrahydro-1H-pyrido[4,3-b]indole compounds. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
CN102188397A Tetracaine hydrochloride multi-vesicular liposome freeze-dried powder and preparation method thereof The invention discloses tetracaine hydrochloride multi-vesicular liposome freeze-dried powder and a preparation method thereof, and relates to a sustained-release preparation of tetracaine hydrochloride. The invention aims to provide the tetracaine hydrochloride multi-vesicular liposome freeze-dried powder with high physical stability and medicament sustained-release effect and the preparation method thereof. The tetracaine hydrochloride multi-vesicular liposome freeze-dried powder comprises the following raw material components in part by weight: 8 parts of tetracaine hydrochloride, 6 to 6.5parts of hydrogenated soybean phosphatidylcholine, 3 parts of cholesterol, 0.1 to 0.2 part of laurin, 5 parts of rosa davurica and 9 to 11 parts of osmotic pressure regulator glucose. The invention also discloses the preparation method of the tetracaine hydrochloride multi-vesicular liposome freeze-dried powder. The freeze-dried powder can be used for preparing local anesthetics.
EP1871360A1 New anti-inflammatory compounds The present invention relates to novel non steroidal anti-inflammatory compounds (NSAIDs) that release hydrogen sulfide (H2S). The present invention also provides methods for treating, preventing and/or reducing inflammation-associated diseases by releasing H2S in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous, or cutaneous systems as well as infective diseases employing said compounds.
US20090036441 Indole Derivatives With Antitumor Activity 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.
US7060691 Pharmaceutical colloidal preparation useful in the treatment of respiratory diseases A pharmaceutical colloidal preparation useful in the treatment of diseases of the upper and lower respiratory tract, and lung parenchyma which contains, as an active ingredient, a colloidal mixture of hyaluronic acids of different molecular weights, in addition to a suitable diluent is described.
US20080038357 Inhalation Powder Containing the CGRP antagonist BIBN4096 and Process for the Preparation Thereof The invention relates to an inhalation powder for treating migraine, containing the CGRP antagonist 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine [BIBN4096] of formula I as the active substance base in the form of spherically nanostructured microparticles, and a process for the manufacture thereof.
WO2012012454A1 Methods of treating metastatic breast cancer with 4-iodo-3-nitrobenzamide and irinotecan Provided herein are methods, compositions and kits for the treatment of locally advanced or metastatic breast cancer or breast cancer brain metastases. The method comprises administration of 4-iodo-3-nitrobenzamide, a metabolite or salt thereof in combination with irinotecan. The method of treating locally advanced or metastatic breast cancer comprises at least one 21 day treatment cycle.
US20100159014 Polymeric micellar clusters and their uses in formulating drugs Polymeric micellar clusters formed from amphiphilic carbohydrate polymers and their uses in formulating drugs is disclosed, and in particular the finding that amphiphilic carbohydrate polymers are capable of self assembling to form micellar clusters in which the carbohydrate amphiphiles aggregate into hierarchically organised micellar clusters of individual aggregates. The micellar clusters may be transformed into stable nanoparticles with drugs, especially hydrophobic drugs that have poor aqueous solubility, and may improve the transfer of hydrophobic drugs across biological barriers.
CN101579320A Sildenafil citrate sublingual tablet and preparation method thereof The invention discloses a sildenafil citrate sublingual tablet and a preparation method thereof. The sildenafil citrate sublingual tablet is prepared from 1 part by weight of sildenafil citrate and 4 to 8 parts by weight of pharmaceutical adjuvant , wherein the pharmaceutical adjuvant comprises 2 to 4 percent of disintegrant, 94 to 96 percent of diluter, 0.5 to 1.2 percent of lubricator, 0.3 to 1 percent of corrective and 0.1 to 0.2 percent of binder, which are based on the total weight of the pharmaceutical adjuvant. Test results show that the prepared sublingual tablet has shorter disintegration time, higher dissolving speed in vitro and higher body bioavailability than the conventional tablets.
WO2013081374A1 Pharmaceutical composition for inhibiting angiogenesis containing plant-derived natural compound The present invention provides a pharmaceutical composition for inhibiting angiogenesis containing a plant-derived natural compound which can be effective for preventing or treating disorders or diseases associated with angiogenesis. The compound used as an active ingredient in the pharmaceutical composition of the present invention suppresses VEGF-induced angiogenic responses without cytotoxicity at a low concentration by inhibiting the expression of an angiogenesis inhibitory factor (for example, VEGF), and thus remarkably improves the safety of a drug.
US7199116 Administering 7-oxo-dehydroepiandrosterone (DHEA) or prodrug incapable of in vivo conversion to testosterone Modulating the metabolism of a dieting mammal by administering to the dieting mammal the metabolic modulating agent 7-oxo DHEA or a pro-drug thereof incapable of in vivo conversion to testosterone.
CN102091065A Application of curcumenol The invention belongs to the technical field of medicine, and discloses a new application of curcumenol in preparation of medicaments for treating human papilloma virus (HPV) infection. By experimental investigation, in multiple factors causing cervical cancer, the invention determines that the curcumenol has a good effect on treating the cervical cancer caused by HPV infection.
CN101683353B Preparation method and application of flavone and flavan derivatives The invention relates to flavone and flavan derivatives contained in medical plant choerospondias axillaries, a preparation method thereof, and an application of the compounds in preparing antihypoxic drugs, antihypoxic health products and other functional foods.
WO2006117299A2 Novel crystalline forms of tiotropium bromide The invention relates to a new crystalline forms of tiotropium bromide, processes for preparing them and their use for preparing a pharmaceutical composition for the treatment of respiratory complaints, particularly for the treatment of COPD (chronic obstructive pulmonary disease) and asthma.
CN101549112A Pharmaceutical composition for treating bad breath and preparation method thereof The invention discloses a pharmaceutical composition for treating bad breath and a preparation method thereof, and the active ingredients of the composition are prepared by extracting more than ten medicinal materials of raw gypsum, reed rhizome, amur corktree bark, dried rehmannia root, white paeony root, honeysuckle flower, bamboo leaf, dwarf lilyturf tuber, immature bitter orange, rhizoma pinellinae praeparata, weeping forsythiae capsule, platycodon root, liquoric root and the like. The unique medicinal active ingredients in the pharmaceutical composition have the efficacies of clearing lung, clearing heat, moistening intestine and relaxing bowels, so that the pharmaceutical composition is used for treating the bad breath caused by improper diet, stomach heat and fumigation.
US20100160310 2,4 (4,6) pyrimidine derivatives The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z1 and Z2 represent NH; Y represents —C3-9alkyl-, —C3-9alkenyl-, —C1-5alkyl-NR6—C1-5alkyl-, —C1-5alkyl-NR7—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-2alkyl-CO-Het10-CO—, —C1-3alkyl-NH—CO-Het3-, -Het4-C1-3alkyl-CO—NH—C1-3alkyl-, —C1-2alkyl-NH—CO-L1-NH—, —NH—CO-L2-NH—, —C1-2alkyl-CO—NH-L3-CO—, —C1-2alkyl-NH—CO-L1-NH—CO—C1-3alkyl-, —C1-2alkyl-CO—NH-L3-CO—NH—C1-3alkyl-, —C1-2alkyl-NR11—CH2—CO—NH—C1-3alkyl-, Het5-CO—C1-2alkyl-, (C1-5alkyl-CO—NH—C1-3alkyl-CO—NH, —C1-5alkyl-NR13—CO—C1-3alkyl-NH—, —C1-3alkyl-NH—CO-Het27-CO—, or —C1-3alkyl-CO-Het28-CO—NH—; X1 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR16—C1-2alkyl-, —CO—NR17—, Het23-C1-2alkyl- or C1-2alkyl; X2 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR18—C1-2alkyl-, —CO—NR19—, Het24—C1-2alkyl- or C1-2alkyl; R1 and R5 each independently represent hydrogen, halo, C1-6alkyloxy- or C1-6alkyloxy- substituted with Het1 or C1-4alkyloxy-; R2 and R4 each independently represent hydrogen or halo; R3 represents hydrogen or cyano; R6, R7, R13, R17 and R19 represent hydrogen; R11 represents hydrogen or C1-4alkyl; R16 and R18 represent hydrogen, C1-4alkyl or Het17-C1-4alkyl-; L1, L2 and L3 each independently represents C1-8alkyl optionally substituted with one or where possible two or more substituents selected from phenyl, methylsulfide, cyano, polyhaloC1-4alkyl-phenyl-, C1-4alkyloxy, pyridinyl, mono- or di(C1-4alkyl)-amino- or C3-6cycloalkyl; Het1, Het2, Het17 each independently represent morpholinyl, oxazolyl, isoxazolyl, or piperazinyl; Het3, Het4, Het5 each independently represent morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl; Het10 represents piperazinyl, piperidinyl, pyrrolidinyl or azetidinyl; Het22 represents morpholinyl, oxazolyl, isoxazolyl or piperazinyl wherein said Het22 is optionally substituted with C1-4alkyl; Het23 and Het24 each independently represent a heterocycle selected from pyrrolidinyl, piperazinyl or piperidinyl wherein said Het23 or Het24 are optionally substituted with Het22-carbonyl; Het27 and Het28 each independently represent a heterocycle selected from morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl.
US20120251638 Nutritional Supplement Comprising Nut Oil Composition The present invention provides a novel composition of nut oils, specifically; walnut oil, almond oil, avocado oil and pistachio oil for use in maintaining and improving health in a convenient and cost-effective manner; for obtaining essential fatty acids that are required for normal body functioning; for reducing cholesterol, and for reducing retinal degeneration in an individual with retinitis pigmentosa.
WO2006057346A1 Ameliorant for renal insufficiency An ameliorant for renal insufficiency which contains as an active ingredient a compound represented by the following formula (1): [wherein R1, R2, and R3 each represents hydrogen or methyl; and X represents C10-28 linear or branched alkylene and alkenylene].
US20060120974 Nicotine delivery systems A delivery system for nicotine including nicotine encapsulated in a microcapsule system which releases the encapsulated nicotine on contact of the microcapsules with a nicotine solvent.
CN1923171B Compound recipe anti-cancer drugs slow release agent comprising anticancer antibiotics and synergist thereof Disclosed is a compound anticancer slow release agent which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slowrelease auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer effective ingredients include Aclarubicin, Idarubicin, Doxorubicin, Epirubicin, Valtaxin, Pirarubicin, Losaxantrone, Losoxantrone and/or anticancer antibiotic synergistic agents selected from phosphoinositide-3-kinase inhibitor, pyrimidine analogues and / or DNA restoration enzymeinhibitor, the slow release auxiliary materials are selected from polylactic acid copolymer EVAc, or sebacic acid copolymer, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C). The slow release microspheres can also be prepared into slow release implanting agent for lowering down the whole body toxicity reaction of the medicament when locally dispensing on the tumor, and for selectively increasing the tumor local medicinal concentration.
CN102389418A Medicine composition containing zafirlukast and statin medicine The invention provides a medicine composition containing zafirlukast and statin medicine and discloses an application of the medicine composition to the preparation of medicine for treating asthma, which belong to the technical field of medicine. Concretely, the medicine composition contains two medicine active ingredients: zafirlukast and 3-oxhydryl-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors according to the mass ratio of 1;(0.01 to 10). In addition, the compound preparation can be made into oral preparations or intestinal tract external preparations.
CN101327216A Atropine sulfate in situ forming eye gel The invention discloses an instant atropine sulphate eye gel and a preparation method thereof. According to the invention, 1000ml of the instant atropine sulphate eye gel contains 1g to 20g of atropine sulphate, 0.05g to 1g of preservative, 1.0g to 7.5g of osmotic pressure adjusting agent, and 30g to 150g of gel stroma, and the rest includes acid-alkali buffer and water for injection. The invention, through the optimization of accessories and the improvement of the technique, enriches the pharmaceutical dosage form of the atropine sulphate, greatly prolongs the time for which the medicine stays in the eyes, and not only improves the curative effect and shortens the time for reaching the function peak, but also reduces the amount of the medicine flowing into and absorbed by dacryocysts and relieves the side effect and toxic reaction of the atropine sulphate.
EP2579871A1 Topical antiviral formulations for prevention of transmission of hsv-2 The present invention relates to formulations of antiviral compounds, in particular [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), suitable for topical application, and to their use in the reduction of or prevention of acquisition and transmission of herpes simplex virus.
CN102961365A Terbutaline sulfate oral instant film and preparation method thereof The invention discloses a terbutaline sulfate oral instant film and a preparation method thereof, and belongs to the technical field of medicines. The terbutaline sulfate oral instant film comprises active ingredients, such as terbutaline sulfate, film-forming materials, disintegrating agents and opacifying agent with effective dosages, and necessary pharmaceutically acceptable filling agents, sweetening agents and wetting agents; and coloring agents are added according to requirements. The terbutaline sulfate oral instant film is good in palatability, fast in response, small in size, and suitable for children, elders, completely-bedridden persons and patients with severe disability; the film can be rapidly dissolved in a disintegrating mode in the oral cavity; water is not needed to orally take; and people can take the medicines any time under a condition that water is inconvenient to drink.
WO2008056156A1 Salts of dihydroxyanthraquinone carboxylic acids and their therapeutic use A compound of general formula (I): wherein Xi is H or COR1 and X2 is H or COR2 but X1 and X2 are not both H; R1 and R2 are the same or different and are each C1-4 alkyl substituted with R3, or a four to seven-membered ring which can be optionally substituted with R8 and can contain one or more additional heteroatoms selected from O, S(O)n and NR9; R3 is F, CF3, OR4, NR5R6 or S(O)nR7; R4, R5 and R6 are the same or different and are each H or C1-4 alkyl optionally substituted with R3, or NR5R6 is a C4-6 heterocycloalkyl ring containing one or more heteroatoms selected from O, NR8 and S(O)n; each n is 0-2; R7 is C1-4 alkyl; R8 is as defined for R3 or C1-4 alkyl optionally substituted with R3 or halogen; R9 is H or C1-4 alkyl; Y is NR9R10R11; and R10 and R11 are the same or different and are each H or C1-6 alkyl optionally substituted with R3 or halogen, or NR10R11 is a four to seven membered ring which can be optionally substituted with R8 or COR1, and can contain one or more additional heteroatoms selected from O, S(O)n and NR9; and hydrates thereof.
US20090036480 5-Ht7 Receptor Antagonists The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some 2,2a,4,5-tetrahydro-1H-3-aza-acenaphthylen substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.
WO2013073382A1 Drug for treatment or prevention of nephropathy Provided is a medical drug having a superior therapeutic or preventive effect against nephropathy. The medical drug is a drug for the treatment or prevention of nephropathy, characterized in comprising as the active ingredient a compound having an α2 adrenaline receptor-blocking effect.
US8815261 Composition for external application comprising aripiprazole and organic acid as active ingredients [Summary] An external preparation formulation superior in the transdermal absorbability has been desired as a new administration route of aripiprazole. Transdermal absorption of aripiprazole has been enabled for the first time by appropriately combining aripiprazole and an organic acid (particularly fatty acid with low lipophilicity). That is, it has been found that more superior transdermal absorbability can be achieved by forming a salt by using a compound showing lipophilicity within the range of −1.5-2, such as fatty acid and the like. It has been further found that the transdermal absorbability is remarkable improved by appropriately selecting the solvent composition. As a result, since a new dosage form of aripiprazole other than oral preparation has been developed, a new transdermal absorption preparation of aripiprazole can be provided.
WO2008119712A1 Benzoimidazole derivatives which have activity at m1 receptor and their uses in medicine Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6 and Q are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
EP2200604A1 Methods of increasing sarcosine levels for treating schizophrenia Methods for increasing sarcosine levels in a patient are provided. The methods include activating the PPARα receptor. Increasing sarcosine levels can be used, for example, as part of a treatment for schizophrenia.
CN102106855A Pharmaceutical preparation for resisting tuberculosis and preparation method thereof The invention relates to a pharmaceutical preparation for resisting tuberculosis, which comprises rifampin, isoniazid, pyrazinamide and ethambutol hydrochloride, wherein the rifampin or the isoniazid is prepared into micropills and residual materials are prepared into granules. According to the invention, one of the rifampin and the isoniazid is prepared into micropills which are separated by isolation gown and the other one is prepared into granules, so that the rifampin and the isoniazid cannot be mutually influenced, the rifampin is ensured to not be basically degraded in the use process, and the bioavailability of the rifampin is improved.
US20090069431 Deuterium-enriched milnacipran The present application describes deuterium-enriched milnacipran, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2012163174A1 Pharmaceutical use of 2-(4-morpholinoaniline)-6-cyclohexyl aminopurine and pharmaceutically acceptable salt or derivative thereof The present invention provides a new use of 2-(4-morpholinoaniline)-6-cyclohexyl aminopurine and pharmaceutically acceptable salt or derivative thereof. The compound can inhibit activated hepatic stellate cells from synthesizing and can express collagen and other extracellular interstitial proteins comprising MMPs and TIMPs, so it can inhibit liver fibrosis; in the body, it can inhibit collagen synthesis and expression, and therefore reverse and treat hepatitis and liver cirrhosis effectively. Also disclosed is a method for preparing drugs for treating or preventing infective hepatitis, non-infectious hepatitis, liver injury, liver cirrhosis, liver cancer and liver fibrosis, and protecting and improving the liver function, in which the compound is used alone or in combination with a target molecule or carrier comprising a vitamin A-coupled liposome.
US20080221085 Nicotinic Receptor Agonists for the Treatment of Inflammatory Diseases Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided.
CN102002050A Bisbenzylisoquinoline derivative and preparation and application thereof The invention relates to a bisbenzylisoquinoline derivative and preparation and application thereof. The derivative has high storage stability and is suitable for preparing medicaments for treating or preventing muscle relaxation, hypertension, amebic dysentery, antianaphylaxis, antipyresis, analgesis and the like of people and animals.
US20060074058 Combination of dpp iv inhibitor and a cardiovascular compound The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and a cardiovascular compound (being different from a statin) or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention, delay of progression or treatment of diseases and disorders selected from the group consisting of hypertension, congestive heart failure, left ventricular hypertrophy, peripheral arterial disease, diabetes, especially type 2 diabetes mellitus, diabetic retinophathy, macular degeneration, cataract, diabetic nephropathy, glomerulosclerosis, chronic renal failure, diabetic neuropathy, syndrome X, premenstrual syndrome, coronary heart disease, angina pectoris, thrombosis, atherosclerosis, myocardial infarction, transient ischemic attacks, stroke, vascular restenosis, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertryglyceridemia, insulin resistance, impaired glucose metabolism, conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, obesity, erectile dysfunction, skin and connective tissue disorders, foot ulcerations and ulcerative colitis, endothelial dysfunction and impaired vascular compliance.
WO2013087544A1 Piperidinyl naphthylacetic acids The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
WO2014031504A1 Novel formulations and uses for curcuma extracts Formulations and uses of extracts of Curcuma longa L. plants for safe use topically, orally, rectally, or vaginally, for example, are provided. A sunscreen containing an extract of Curcuma longa L. is provided, the sunscreen having an absorption that spans the UVA and UVB ranges in a manner that meets updated FDA recommendations without requiring the addition of titanium dioxide. A process of producing the extract is also provided, using an extraction solvent that is at least substantially non-toxic and useful also as a pharmaceutically acceptable carrier in liquid dosage forms. The extraction process also produces a significantly higher yield from a single extraction than the state-of-the-art. Liquid dosage forms can be produced directly from the extraction process without requiring removal of the extraction solvent, reducing complexity and cost of processing over the state-of-the-art. Microemulsions and nanoemulsions are also provided to enhance the bioavailability and stability of the extracts.
CN103159691A Preparing method and application of isothiocyanate compound The invention relates to a preparing method and application of isothiocyanate compound and particularly provides the isothiocyanate compound which has a structure showed in the following general formula (I). The isothiocyanate compound is capable of restraining survival and growth of cells of KG1a, MCF-7, K562, HCC1954, SUM159 and the like, wherein R is: R1 is: C1, Br or alkyl; n = 0, 1, 2.
EP1954322A2 Mitochondria-targeted antioxidant prodrugs and methods of use The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.
US20090099208 Novel guanidine derivatives and their medical use This invention relates to novel guanidine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
US20080194522 Substituted benzopyran-2-ones; competitive binding ligands for MAO inhibition; anxiolytic agents; neurodegenerative diseases, nervous system disorders; drug screening by comparing detectable changes in fluorescence when samples are oxidatively deaminated in the presence of a MAO The present invention relates to compounds useful for detecting the activity of monoamine oxidases, compounds useful for competitively inhibiting monoamine oxidases, for determining inhibitors of monoamine oxidases and compounds useful for treating monoamine oxidase-related nervous system pathologies, as well as pharmaceutical compositions and methods of manufacture thereof.
EP2459553A1 Furazanobenzimidazoles as prodrugs to treat neoplastic or autoimmune diseases A compound of formula (II) wherein (a) represents a divalent benzene residue which is unsubstituted or substituted by one or two additional substituents independently selected from lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, mono(lower alkyl)amino, di(lower alkyl)amino, mono(lower alkenyl)amino, di(lower alkenyl)amino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower 15 alkoxycarbonyl, cyano, halogen, and nitro; or wherein two adjacent substituents can be methylenedioxy; or a divalent pyridine residue (Z = N) which is unsubstituted or substituted additionally by lower alkyl, lower alkoxy, lower alkoxy-lower alkoxy,amino, optionally substituted by one or two substituents selected from lower alkyl, lower alkenyl and alkylcarbonyl, halo-20 lower alkyl, lower alkoxy-lower alkyl, or halogen; R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkylor cyano-loweralkyl; and R2 represents a group selected from: (b), (c) and (d); or pharmaceutically acceptable salts thereof.
WO2007060458A2 Treatment of ophthalmic diseases with beta-amino alcohols Beta-amino alcohols are useful for the treatment of ophthalmic conditions.
CN101948500A New derivative of camptothecin 20-site coupled bile acid The invention relates to camptothecin derivatives shown in formula I and II and a drug thereof, in particular to a method for preparing compounds of the invention and an application of compounds as drugs in curing rumours. In the formula I and II, R1 is hydrogen and ethyl, R2 is hydrogen and nitryl, R3 and R4 are hydrogen, hydroxide radical and carbonyl, and R5 is hydroxide radical and carbonyl.
CN1919290A Decoction medicine for treating urethritis of lumbago type and its preparing process Disclosed is a medicinal broth for treating lumbago type urethritis and its preparing process, wherein the medicament is prepared from the following raw materials (by weight portion): coix seed 25-30g, knotgrass, honeysuckle flower, lysimachia christinae each 18-20g, rhubarb horsetails, Chinese pink herb, achyranthes and cyathula root, Loranthus parasiticus each 12-15g, plantain seeds, talcum, cape jasmine, clematis stem, rush pith, poria cocos wolf each 8-10g, and licorice root 5-7g. The invention realizes easy material availability, simplified preparation, low cost, and quick effect.
CN103720650A Baicalin injection with anti-influenza virus effect The invention relates to a baicalin injection with anti-influenza virus effect, which is prepared from baicalin weighed according to required volume and set concentration, 0.6g of sodium dihydrogen phosphate, 2.16g of disodium hydrogen phosphate and 100ml of injection water through high-temperature high-pressure sterilization, wherein the pH value of sodium hydroxide is regulated to 7.0. The medicine has a remarkable advantages of in-vivo and in-vitro anti-influenza virus activity, high bioavailability, small side effect and adverse response and the like, has the effect of inhibiting neuraminidase activity to stop virus release, has unique advantages and wide development prospect in the field of preventing and treating influenza virus.
WO2008135767A1 New triazole compounds useful in the treatment of inflammation There is provided compound formed by an association between: (i) a compound of formula (I), wherein at least one of the substituents X1 and X2 on the phenyl ring represents (independently) F, Cl, OCF3, CF3, CHF2Or OCHF2; and (ii) a metal, an organic amine or a basic amino acid. Such compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.
CN103315999A Compound amino acid composition and preparation method thereof The invention relates to a pharmaceutical composition, and particularly relates to a compound amino acid composition and a preparation method thereof. The compound amino acid composition contains 18 amino acids and pharmaceutical adjuvants; tryptophan is a compound as shown in an X-ray powder diffraction figure I, which is obtained by measurement with a Cu-Kalpha ray. The preparation of the compound amino acid composition, which is prepared from the tryptophan, has good stability and is very suitable for clinical application. The compound amino acid composition has very good mobility and is convenient for preparing the preparation in the medicine preparation process.
EP2446881A1 Orally Dissolving Films Rapidly dissolving, oral film preparations for rapid release of an active agent in the oral cavity, in particular, rapidly dissolving oral films comprising a nicotine active which achieve good transbuccal absorption and provide nicotine craving relief to an individual are disclosed herein.
CN101108194B Method of eliminating sodium chloride in iron-dextran complex compound water solution and device thereof The invention relates to a method and device for eliminating sodium chloride in the aqueous solution for the complex of ferrodextran, which is characterized in that: the ferrodextran is prepared with dextran and ferric trichloride. The sodium chloride in the ferrodextran is eliminated with an electrodialysis film, that is, eliminating the sodium chloride of the solvent by electrodialysis process in the ferrodextran complex solvent with iron content is more than or equal to 40mg/ml, sodium chloride content is more than or equal to 5.0 per cent wt and viscosity of 3.0mpa is multiplied by s (20 DEG C.) under the temperature of 10 to 90 DEG C. Compared with the technique of eliminating sodium chloride with alcohol precipitation, the invention prevents the safety hazard from flammable and combustible alcohol and reduces the production cost.
CN102145045A Externally-applied weight reducing drug The invention discloses an externally-applied weight reducing drug, consisting of the following raw materal drugs in parts by weight: 30-40 parts of ligusticum wallichii, 30-40 parts of herba eupatorii, 30-40 parts of radix angelicae sinensis, 20-30 parts of eucommia bark, 20-30 parts of angelica dahurica, 20-30 parts of frankincense, 10-30 parts of myrrh, 15-25 parts of rhizoma atractylodes, 15-25 parts of radix angelicae pubescentis, 2-5 parts of flos caryophylli, and 2-5 parts of borneolum syntheticum. The preparation method comprises the following steps of: mixing the components except for the borneolum syntheticum; adding water in the mixture and immersing; decocting with slow fire for 1-1.5 hours; filtrating and eliminating filter residues; drying the filtered liquid; obtaining an extract; grinding the extract into fine powder; and mixing the fine powder with the borneolum syntheticum which is ground into powder; mixing evenly and obtaining the drug. The drug in the invention has the functions of nourishing blood and activating blood circulation, eliminating dampness and dredging channels, invigorating stomach and removing food stagnation, supporting Yang and diminishing swelling and the like. The practice shows that the externally-applied weight reducing drug has dramatic weight reducing effect without toxic and side effects.
US20120073508 Insulin-like gene in prawns and uses thereof The present invention relates to a nucleic acid molecule encoding an insulin-like factor of the androgenic gland of the freshwater prawn Macrobrachium rosenbergii (M. rosenbergii). The present invention further relates to methods of silencing the expression of the insulin-like factor gene in decapod crustaceans order, particularly in M. rosenbergii, useful for producing male monosex populations.
CN102697916A Medicine for alleviating hangover The invention discloses a medicine for alleviating a hangover. The medicine is prepared from the following raw materials in parts by weight: 3-4 parts of pueraria lobata ohwi, 4-5 parts of mung bean, 4-5 parts of vivipara, 2-3 parts of raisin tree seed, 2-3 parts of lignum cinnamomi camphorae, 2-3 parts of persimmon, 1-2 parts of pericarpium citri reticulatae and 2-3 parts of white sugar. A preparation method for the medicine for alleviating the hangover comprises the step of grinding the raw materials into a powder. The medicine for alleviating the hangover has a function of rapidly alleviating the hangover well, i.e. drunk drinkers can be totally sobered after 1-2 hours by taking 3-5g of the medicine a time, and the drinkers can also take the medicine with water before drinking or during drinking or after being drunk, and thus, the hangover is prevented before the drinkers drink, the drinkers are sobered during the drinking, and the hangover is alleviated after the drinkers are drunk.
CN102600141A Dispersible tablet containing amoxicillin and potassium clavulanate The invention belongs to the technical field of western medicine preparations, and particularly relates to a dispersible tablet containing amoxicillin and potassium clavulanate. The dispersible tablet comprises the following components in parts by weight: 420 parts of amoxicillin, 60 parts of potassium clavulanate, 350-400 parts of filler, 80-100 parts of low-substituted hydroxypropyl cellulose, 1-20 parts of colloidal silicon dioxide and 5-8 parts of magnesium stearate. For the dispersible tablet, both the dispersing uniformity and dissolution achieve the technological effects of the existing product, simultaneously, and the hardness of the pressed tablet is within 50-70N, so that the problems of insufficient hardness and difficulty in common packaging existing in products on the market are solved.
WO2010039040A1 Composition comprising a ppar agonist and a phospholipid component The present invention relates to compositions comprising at least one peroxisome proliferator-activated receptor (PPAR) agonist and a lipid component. Such compositions are particularly suitable for the prophylaxis and/or the treatment of conditions associated with insulin resistance and/or glucose intolerance and/or hyperglycemia.
EP1688137A1 SPM 927 for add-on therapy of schizophrenia The present invention is directed to the use of a class of peptide compounds for treating schizophrenia in an add-on therapy.
WO2006106995A1 Matrix metalloproteinase inhibitor comprising ingredient extracted from amula [PROBLEMS] To provide a novel matrix metalloproteinase (MMP) inhibitor having an excellent inhibitory effect on an MMP activity. [MEANS FOR SOLVING PROBLEMS] An MMP inhibitor comprising an ingredient produced by extracting a fruit of amula (Emblic officinalis Gaertn.) with a solvent; and a composition for oral use, food or cosmetic comprising the MMP inhibitor.
CN101327181A Puerarin in situ forming eye gel The invention discloses a puerarin instant eye gel and a preparation method thereof. 1000ml puerarin instant eye gel of the invention contains 2g to 30g of puerarin, 0.05g to 1g of antiseptic, 1.0g to 7.5g of osmo-regulator, 30g to 150g of gel matrix and rest of buffer solution and injection water. Proved by clinical practice, the invention has advantages of perfect effect of anti-glaucoma, safe and convenient use, less side effect, eyesight protection, etc. Primary angle-closure glaucoma is one of serious nonreversible diseases causing blind. China is the high risk region for angle-closure glaucoma, the illness frequency rate thereof is fourteen times higher than that of Occident. The peripheral iridectomy is mainly used to prevent intraocular pressure elevation in early period. Preliminary experiment proves that the invention has certain curative effect on primary angle-closure glaucoma.
US20100168145 Fused imidazole derivatives and use thereof as aldosterone synthase inhibitors The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R1, R2, X, Y, Z, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
US20100278824 Combinations comprising gemcitabine and tyrosine kinase inhibitors for the treatment of pancreatic cancer The invention relates to a method of treating a warm-blooded animal having pancreatic cancer, in particular it relates to a method comprising administering to the warm-blooded animal having pancreatic cancer a dual inhibitor of the epidermal growth factor receptor (EGF-R) tyrosine kinase activity and the vascular endothelial growth factor receptor (VEGF-R) tyrosine kinase activity, to a method comprising administering to the warm-blooded animal having pancreatic cancer a combination comprising (a) a compound which decrease the activity of the EGF and (b) a compound which decreases the activity of VEGF, to a combination comprising (a) a dual inhibitor of the EGF-R tyrosine kinase activity and the VEGF-R tyrosine kinase activity or, alternatively, a compound which decrease the activity of the EGF and a compound which decreases the activity of VEGF and (b) at least one compound selected from an inhibitor of the platelet derived growth factor receptor (PDGF-R) tyrosine kinase activity and antineoplastic anti-metabolites; to a method of treating a warm-blooded animal having pancreatic cancer comprising administering to the warm-blooded animal said combination; to the use of such a combination for the preparation of a medicament for the treatment of pancreatic cancer; and to a commercial package or product comprising such a combination together with instructions for the treatment of pancreatic cancer.
CN101822801A External Chinese patent drug for treating tubal obstruction barrenness and preparation method thereof An external Chinese patent drug for treating tubal obstruction barrenness and a preparation method thereof relate to the technical filed of medical preparation derived from plant materials in International Classification A 61K. The complete formula of the invention consists of motherwort, red paeony root, zedoary, radix angelicae, cinnamon and camphor. The raw materials are purified through enzymolysis oligopeptides and is processed into small molecules. The purified superfine powder is mixed according to a certain proportion, blended into various preparation forms and made into finish product in different packages. The method treats diseases through external administration by dipping hands and feet and covering bellybutton, lower abdomen and other points. The invention achieves the aims of relieving visible and invisible dropsy among tissues around fallopian tube and nonsterile and sterile inflammatory excrescence hyperplasia through the sense and absorption of hand and foot peripheral nerves and blood circulation. The invention has the advantages of simple operation, quick response due to targeting drug delivery, low cost and obvious effect.
CN1895254A Gynopathic effervescent tablets and production thereof A vaginal effervescent tablet of ofloxacin for treating gynopathy is prepared through adding ofloxacin to the effervescent foaming agent consisting of acid system formed by acid or acidic salt and alkali system formed by carbonate, adding foam stabilizer and filler, stirring, granulating, baking, and die pressing.
WO2011097946A8 Oxazolidinone compounds containing ring-fused bicyclic ring, preparation method and use thereof Oxazolidinone compounds containing ring-fused bicyclic ring represented by the general formula (I), pharmaceutically acceptable salts and stereoisomers thereof are disclosed, wherein R1, R2, R3, R4, R5, R6, and -Y- are defined as in the description. Also disclosed are the preparation methods of such compounds, pharmaceutical compositions and pharmaceutical preparations containing the same and uses of the same in the manufacture of medicaments for treating and/or preventing infectious diseases, and in the treatment and/or prevention of infectious diseases.
US20080146657 Plant-Origin Alpha3-Adrenoceptor Agonist and Use of the Same The present inventors produced lotus leaf extracts, and discovered that quercetin is one of the active ingredients. As a result of treating β3-adrenergic receptor-expressing cells and feeding diabetes model mice with quercetin and evaluating its effects, the present inventors discovered specifically that quercetin produces obesity-improving effects and antidiabetic effects by acting as a β3-adrenergic receptor agonist.
CA2631128A1 Tricyclic amide derivatives useful for treating obesity The present invention relates to compounds of formula (I) wherein A, G, r and R1 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
US6977076 Immunomoderators; high molecular weight polysaccharides Chlorella extracts containing high molecular weight Chlorella polysaccharide and polysaccharide complexes show immune modulatory, specifically immune stimulatory, activity. The polysaccharide and polysaccharide complexes contain glucose and any combination of: galactose, rhamnose, mannose and arabinose, as well as N-acetyl glucosamine and N-acetyl galactosamine. The extracts may be treated with pronase, DNAse, RNAse and proteases to remove unassociated nucleic acids, ribonucleic acids and proteins. The extracts may also undergo treatment to effect cleavage of specific glycosidic linkages, the linkages being defined by their susceptibility to cleavage by amylase, amyloglucosidase, cellulase or neuraminidase. Chlorella extracts may be administered to a mammal to increase proliferation of splenocytes and increase production of cytokines such as IL-6, IL-10, INF-γ and TNF-α. They may be used as a supplement to a vaccination regimen.
US7276510 Viricides; prevent reproduction of human T-Cell lymphocyte virus This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, provided that when Q is halo then Z is N; or when Q is polyhaloC1-6alkyl then Y is hydrogen or C1-6alkyl; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
CN102212001A Compound salvianolic acid F methyl ester and preparation method thereof The invention discloses a novel compound, namely salvianolic acid F methyl ester which is obtained by carrying out thermal decomposition on total salvianolic acid and has the activities of resisting reperfusion injury and resisting platelet aggregation. The compound has obvious antioxidation, has an obvious protective function on myocardial ischemia reperfusion injury of a rat and simultaneously has activity of resisting platelet aggregation. According to the invention, a lead compound is provided for developing a novel medicament which is used for treating ischemic cerebrocardiac diseases.
WO2011137428A1 Methods of treating hiv infection: inhibition of dna dependent protein kinase Methods of treating HIV-1 infection/ AIDS in a patient infected with an HIV-1 virus comprising providing a DNA-PK inhibitor to the patient are provided herein. In one embodiment the DNA-PK inhibitor is compound of the Formula I (shown in the specification) or a pharmaceutically acceptable salt thereof. Methods of inhibiting CD4 cell death are also provided.
US7557110 Pyrazolo[1,5-A] pyrimidine derivatives The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent kinase inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for a protein kinase mediated disorder in which kinase is implicated, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.
WO2013049521A3 Light-enabled drug delivery Conjugates are provided which comprise a membrane permeable drug linked to a moiety that is not membrane permeable. Attachment of the moiety that is not membrane permeable prevents the drug from crossing cell membranes and entering cells. However, exposure to light either i) breaks the linkage, releasing the drug and allowing it to enter cells; or ii) converts the non-membrane permeable moiety to a membrane permeable form, allowing the entire conjugate to enter the cell, where the drug is released from the conjugate by cleavage. The membrane permeable drugs are thus delivered to cells at locations of interest, e.g. cancer cells in a tumor, in a temporally and spatially controlled manner.
CN103251583A Application of quercetin in drug for preventing and treating acute radiation pneumonitis and preparation prepared from quercetin The invention discloses application of quercetin in a drug for preventing and treating acute radiation pneumonitis and a preparation prepared from the quercetin. The quercetin can be used for remarkably improving inflammatory exudation of mice radiation-induced pulmonary injury lung tissue, has a certain preventing and treating effect for the radiation-induced pulmonary injury, so that a novel material drug is provided for treating the acute radiation pneumonitis.
WO2008043263A1 Isoxazole derivatives and methods of treating diseases A series of isoxazole derivatives and methods of treating immune-mediated diseases by isoxazole derivatives are described.
US20050215549 TACE inhibitors A compound of the formula wherein R1, R2 R3, R4, R5, R6 and Q are as defined above, useful in the treatment of arthritis, cancer, and other diseases involving the dysregulated production/release of reprolysins such as TNF and other diseases characterized by matrix metalloproteinase activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID's), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
US20100189757 Drug depot implant designs and methods of implantation The present invention relates to novel drug depot implant designs for optimal delivery of therapeutic agents to subjects. The invention provides a method for alleviating pain associated with neuromuscular or skeletal injury or inflammation by targeted delivery of one or more therapeutic agents to inhibit the inflammatory response which ultimately causes acute or chronic pain. Controlled and directed delivery can be provided by drug depot implants, comprising therapeutic agents, specifically designed to deliver the therapeutic agent to the desired location by facilitating their implantation, minimizing their migration from the desired tissue location, and without disrupting normal joint and soft tissue movement.
CA2747938A1 Immunostimulating saponins for use in in situ tumor-destruction therapy The present invention relates to pharmaceutical compositions for use in in situ tumor- destruction therapy compris-ing the steps of tumor destruction and administration of an immunostimulating amount of an immunopotentiator, and to the use of such pharmaceutical compositions in the manufacture of a medicament.
WO2011139763A1 Methods and compositions for inducing satiety The present invention provides a medicament or food supplement, that when ingested by an individual, forms a gel mass in the individual's stomach, said gel mass consisting essentially of methylcellulose and water, as well as methods for inducing satiety, reversibly reducing stomach void volume, and reducing caloric intake in an individual.
US20110301225 Compounds and Methods for Reducing the Recruitment and/or Migration of Polymorphonuclear Cells A therapeutically effective amount of an oligonucleotide is capable of influencing the properties and behaviour of polymorphonuclear cells, e.g. suppressing endothelial adhesion and transmigration of said cells, and through this mechanism reduce the recruitment and/or migration of polymorphonuclear cells to a site of inflammation.
EP1507757A1 Lactams used as anti-viral agents The invention relates to lactams, to methods for producing the same and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for use as anti-viral agents specifically against cytomegaloviruses.
CN103099936A Cough relieving medicine The invention discloses a cough relieving medicine for treating various coughs. Different from the prior art, the design scheme is as follows: the cough relieving medicine is prepared by proportioning fresh garlic head, white pepper powder, benproperine clenbuterol and dexamethasone by percents of (10-20): (5-10): (0.05-0.1): (0.0001-0.0002): (0.02-0.03), grinding, uniformly mixing and sealing. The cough relieving medicine has the advantages of good effect, remarkable cough relieving effect, and is convenient to use, and is used for treating coughs caused by cold, trachitis, pneumonia, phthisis and the like.
WO2007058960A1 Sulfamoyl benzamides as cannabinoid receptor modulators Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.
WO2010083280A3 Methods for treating obesity and disorders associated with hyperlipidemia in a mammal The disclosure relates to methods for treating hyperlipidemia in a mammal. The present disclosure also relates to methods for treating and/or controlling obesity in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, AEGR-733 and implitapide) and a DGAT inhibitor (for example, JTT- 553 or PF-04415060). Co-administration of the MTP inhibitor with the DGAT inhibitor produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit.
EP1709018B1 Acylaminothiazole derivatives and use thereof as beta-amyloid inhibitors The invention relates to a compound having general formula (I), wherein: R1 represents either an optionally-substituted C1-6 alkyl or a C3-7 cycloalkyl, a thiophene, a benzothiophene, a pyridinyl, a furanyl or a phenyl, said phenyl groups being optionally substituted; R2 and R'2 represent, independently of each other, a hydrogen atom, a halogen atom, a hydroxy, a C1-3 alkoxy, a C1-3 alkyl, a C3-7 cycloalkyl, an O-C(O)-C1-6 alkyl group, or R2 and R'2 together form an oxo group; R3 represents either a hydrogen atom or an optionally-substituted C1-6 alkyl; R4 and R5 represent, independently of each other, a hydrogen atom, a C1-7 alkyl, a trifluoromethyl, an L group or a Z group; G represents a C1-7 alkyl or a single bond; M represents a C3-7 cycloalkyl, a phenyl, a naphtyl or a pyridinyl, group M being optionally substituted; J represents a hydrogen atom or a group -Y-K; Y represents a single bond, an oxygen atom, a sulphur atom, an optionally-substituted -C1-4 alkylene- group, -O-C1-4 alkylene-, -C1-4 alkylene-O- or -N(W)-; K represents a phenyl or pyridinyl group, group K being optionally substituted, with the proviso that at least one R4 or R5 group represents a Z group; and Z represents a group CN, SO2NR6R7, or a heteroaromatic group, said heteroaromatic group being optionally substituted. The inventive compound takes the form of a base, an acid addition salt, a hydrate or a solvate. The invention also relates to the use of said compound in therapeutics.
EP1561464A2 Use of cyclopamine in the treatment of basal cell carcinoma and other tumors The present invention is directed to the use of a derivative of cyclopamine for the manufacture of a medicament for obtaining decreased size or disappearance of a tumor employing hedgehog/smoothened signaling for the prevention of apoptosis and/or for the prevention of differentiation of tumor cells, wherein said medicament is to be administered in an amount which induces differentiation and apoptosis of said tumor cells.
WO2010136847A1 Coated metformin with pioglitazone solution The present invention relates to coating of biguanide antihyperglycaemic agents (such as metformin hydrochloride) with solution of insulin sensitizers (such as thiazolidinediones; pi- oglitazone hydrochloride).
CN102351835A Mangiferin aglycone crystal forms, and composition, preparation method and application thereof The invention relates to the field of pharmaceutical chemistry, and discloses mangiferin aglycone crystal forms I and II, and a pharmaceutical composition, preparation method and application thereof. The mangiferin aglycone crystal form I or crystal form II provided by the invention has the advantages of single crystal form, high purity, high stability, high solubility and high bioavailability, can lower the serum uric acid concentration, and can be used for preparing medicines for preventing and treating hyperuricemia. The preparation method of the mangiferin aglycone crystal form I or crystal form II has the advantages of accessible raw materials and low production cost, and is suitable for industrial production.
US20070265194 Agents for the treatment of viral infections The invention relates to methods of treating a hepatitus virus infection by administering a therapeutically effective amount of a proteasome inhibitor and a pharmaceutically acceptable carrier to a subject in need thereof. Preferably, the protesome in hibitor inhibits or regulates a ubiquitin proteasome pathway.
WO2008030512A3 Polystyrene sulfonate polymer tablets, their preparation and use The present invention provides tablets containing at least about 70% of polystyrene sulfonate polymer, binder and moisture. The invention further relates to methods of treating medical conditions including antibiotic-associated diarrhea such as that caused by Chlostridium difficile, comprising administration of the tablets to a subject in need thereof. Furthermore, pharmaceutical blends and methods of preparing the tablets are disclosed.
WO2012004604A1 Tetrazole compounds as calcium channel blockers The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial. Formula (I) wherein A is: (II) or (III)
CN103242318A Salt of triazole-pyridazine derivative The invention relates to 6-{difluoro-[6-(1-methyl-1H-pyrazole-4-yl)-[1,2,4] triazole [4,3-b] pyridazine-3-yl] methyl}-quinoline and a derivative fumarate or a pharmaceutically acceptable solvate thereof, and an application thereof in preparation of medicines for treating cancers.
US20080262010 dissolving with D-glucoronic acid in one or more solvents; and precipitating one crystalline polymorph as the D-glucoronate salt; kinase-inhibiting The present invention relates to methods for preparing one or more crystalline polymorphs of a compound of formula I: and structurally related compounds. The present invention is also directed to methods for converting one polymorph to other different polymorphs of formula I and structurally related compounds.
US20070276004 Pharmaceutical Composition Comprising an Immunosuppressant for Use in the Treatment of Skin Diseases Synergistic combinations of a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro-33-desoxyascomycin and an emollient such as dimethicone, glycerol or isostearyl isostearate are provided, which are useful in particular in the treatment of dermatological or mucosal diseases such as dry skin or atopic or contact dermatitis.
CN1640396A Novel medicinal compositions The present invention relates to a new medicine composition, it is an injection preparation containing water-soluble vitamin and amino acid. Said injection preparation can be used for curing various diseases resulted from deficiency of vitamin and amino acid.
CA2839869A1 Anti-erbb3 antibobies in combination with paclitaxel for treatment of gynecological cancers Provided are methods and compositions for clinical treatment of advanced gynecological cancers using anti-ErbB3 antibodies combined with paclitaxel.
CN101669950A Application of aloperin in preparation of drug for treating ulcerative colitis The invention relates to application of aloperin in preparation of drug for treating ulcerative colitis. The inventor finds that the aloperin has the effect of treating ulcerative colitis and can be applied to preparation of drug for treating ulcerative colitis. The invention also provides a colon target preparation of aloperin, aiming at better effect of ulcerative colitis treatment. The preparation is composed of tablet core and retardant layer wrapped outside the tablet core, and the mass ratio of the tablet core and the retardant layer is 1:1-0.4; wherein the tablet core is composed of 10-70% of aloperin, 10-80% of guar gum and 5-30% of dextrin by percent of the total mass of the tablet core, the retardant layer is the guar gum. The target preparation of the invention can be specifically dissolved and release aloperin at colon part, so that the aloperin can be dispersed in the whole colon at higher concentration, thus effectively improving the effect of aloperin for treating ulcerative colitis.
US20120232162 Use of lutein containing compositions to improve certain aspects of memory This invention relates to a method of enhancing an aspect of memory in a healthy individual, wherein the aspect of memory is selected from the group consisting of: associative memory, spatial memory and memory under stress comprising: administering a composition consisting of: a) an effective amount of either lutein or the combination of lutein and zeaxanthin; and b) an appropriate carrier; and observing the enhanced associative memory, spatial memory or memory under stress.
WO2006023295A3 Pharmaceutical compositions comprising effervescent agents and fenofibrate A pharmaceutical composition comprising at least one effervescent agent and a fibrate and a process for making such composition. The fibrate is fenofibrate and the effervescent agent are in a dosage form. The dosage form increases dissolution and absorption of fenofibrate in biological conditions where the form contacts acidic gastric fluid after oral administration.
EP1192125B9 Mono-substituted 3-propyl gamma-aminobutyric acids The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula (I). The compounds are useful as therapeutic agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, arthritis, sleep disorders, IBS, and gastric damage. Methods of preparing the compounds and useful intermediates are also part of the invention.
CN102138916B Levo-gossypol for treating tumors or cyclodextrin clathrate compound of acetate thereof The invention discloses levo-gossypol for treating tumors or a cyclodextrin clathrate compound of an acetate thereof, which consists of levo-gossypol or a levo-gossypol acetate, polyethylene glycol and hydroxypropyl-beta-cyclodextrin, wherein the polyethylene glycol is one of polyethylene glycol 1500 or polyethylene glycol 2000; a mass ratio of the levo-gossypol or the levo-gossypol acetate to the polyethylene glycol is 1:(0.3-1.2); the average substitution degree of the hydroxypropyl-beta-cyclodextrin is between 4.6 and 6.5; and a mass ratio of the levo-gossypol or the levo-gossypol acetate to the hydroxypropyl-beta-cyclodextrin is 1:(7.0-12.0). The levo-gossypol for treating the tumors or the cyclodextrin clathrate compound of the acetate thereof has the advantages of high bioavailability and stability, large medicine carrying amount and the like.
WO2007115473A1 Pyrrole derivatives inhibitors, their curative uses The present application discloses 2-acetamido-3-carbomethoxy-5-(6,7-dihydro- 6-oxo-4-arylamido pyrrolo[2,3-d]pyrimidine –5-)methylene-1H-pyrrole derivatives of general formula (I),processes for their preparation, the pharmaceutical compositions containing them and their uses as therapeutic agents especially as protein kinase inhibitors. The definitions of substituents in formula (I) are the same as description.
WO2013033981A1 2,7-naphthyridine derivative, preparation method therefor and use thereof Disclosed are a 2,7-naphthyridine derivative, preparation method therefor and use thereof, with the structure as the compound represented by formula (I), a pharmaceutically acceptable equivalent or salt. The compounds having the structure represented by formula (I) according to the present invention have a high inhibitory effect on activity of many kinases, with IC50 for the kinases such as c-Met, KDR and c-kit being less than 10-7 mol.L-1 generally. Meanwhile, the compounds having the structure represented by formula (I) prepared in the embodiments of the present invention have an inhibitory effect on proliferation of a variety of tumor cells. In addition, the present invention also relates to an intermediate of the compounds and preparation method therefor.
EP1792989A1 13 Transmembrane protein expressed in prostate cancer A prostate tumour associated gene (designated 24P4C12) and its encoded protein is described. 24P4C12 is highly expressed in prostate tissue xenografts, providing evidence that it is turned on in at least some prostate cancers. 24P4C12 provides a diagnostic and/or therapeutic target for prostate and other cancers,
CN102675244A Thiazine amide derivative and application thereof in preparation of medicines for preventing and controlling neurodegenerative diseases The invention relates to a compound shown as the formula I, pharmaceutically acceptable salts of the compound, and/ or solvates and/ or hydrates of the compound. The invention also relates to a preparation method of the compound, a medicinal composition containing the compound, and application of the compound in preparation of medicines for preventing and controlling neurodegenerative diseases. In the formula I, R1 is hydrogen or linear-chain or branched paraffin containing 1-4 carbon atoms, and R2 is linear-chain or branched paraffin containing 1-4 carbon atoms, or linear-chain or branched paraffin which contain 1-4 carbon atoms and is substituted by benzene ring.
EP1712554A1 Pyridobenzoxazine derivative A quinolone antimicrobial agent having potent antimicrobial activity against gram positive and gram negative bacteria and having high safety is provided. A compound represented by the following formula (1): [wherein, R1: hydrogen, alkyl, cycloalkyl, or substituted carbonyl derived from amino acid, peptide or tripeptide; R2: hydrogen, alkyl, or cycloalkyl; R3: hydrogen, amino, halogen, or alkyl; R4: hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, ethoxycarbonyl, choline, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, alkyl, alkoxymethyl, or phenylalkyl; X, X1, X2: hydrogen or halogen] or salt thereof, or a hydrate thereof; and antimicrobial agent and therapeutic agent for infections, each containing the compound, salt thereof or a hydrate thereof.
CN102512398A Simvastatin osmotic pump preparation and preparation method thereof The invention discloses simvastatin monolayer osmotic pump sustained release tablets. Each simvastatin monolayer osmotic pump sustained release tablet comprises a tablet core and a controlled-release film coated layer, wherein the tablet core contains the following components in percentage by weight: 1 to 20 percent of simvastatin serving as a main medicine, 1 to 25 percent of filling agent, 50 to 90 percent of penetrating agent, 1 to 15 percent of adhesive, 0.5 to 5 percent of release conditioning agent and 0.5 to 3 percent of lubricating agent; the controlled-release film coated layer comprises a controlled-release film-forming material, a plasticizer and/or a pore-forming agent; the filling agent comprises microcrystalline cellulose and dextrin; and the penetrating agent contains cane sugar and lactose.
WO2014088087A1 Double-stranded ribonucleic acid for adjuvants The present invention provides: double-stranded ribonucleic acid (dsRNA) which has a chain length suitable for exhibiting a high function and low toxicity in use applications such as adjuvants, and rarely undergoes the change in chain length even when subjected to a heating/cooling treatment, or a salt of the dsRNA; an immunostimulating substance, an adjuvant, a medicine or the like which contains the dsRNA or the like; and a method for producing the dsRNA or the like. The present invention is characterized in that the weight average chain length of each of at least two strands of single-stranded ribonucleic acid (ssRNA) which constitute a first chain constituting the dsRNA is 1/2 or shorter of the weight average chain length of a strand of ssRNA which constitutes a second chain constituting the dsRNA.
CN102600120A Application of cinnamic acid in preparation of drugs for preventing and treating livestock and poultry virus infection The invention relates to application of cinnamic acid in the preparation of drugs for preventing and treating livestock and poultry virus infection. Cinnamic acid has an activity resisting to poultry virus diseases, and can effectively prevent and treat infections of a bird flu H9 subtype virus, a bird flu H5 subtype virus, an infectious bursal disease virus LX strain, a nephropathogenic infectious bronchitis virus and an avian infectious laryngotracheitis virus, so that the death rate of diseased chickens is reduced, the survival rate of the poultry is effectively increased and the parturition performance of the poultry is effectively improved.
US20060178356 Treating oxidative stress-related conditions typically responsive to cellular enzyme modulation with a substituted phenolic compound having unsaturated groups, e.g. 1-((3-methyl-5-oxo-2-pyrazolin-1-yl), 4-(3-methoxy-4-hydroxy-phenyl)-vinyl-)benzene; skin disorders; antiischemic and cardiotonic agents Cytoprotective compounds, many of which are phenolic derivatives characterized by a substituted phenol having certain conjugated bonds, are useful in the treatment of certain ischemic or inflammatory conditions, including but not limited to stroke, myocardial infarction, congestive heart failure, and skin disorders characterized by inflammation or oxidative damage. They are also useful in the manufacture of pharmaceutical and cosmetic formulations for the treatment of such conditions.
US20120316134 Anaesthetic composition A stable anaesthetic composition is described which is particularly suitable for use in cats and dogs. The composition comprises an aqueous solution of an anaesthetically effective amount of water soluble cyclodextrin or a cyclodextrin derivative complex of alfaxalone and a bugger, excluding phosphate buffer pH 7.0, 0.1 M mixed as defined in the British Pharmadopoeia 1998, such that the pH of the solution is from 6.0-8.0.
CN101978993A Composition for nourishing and blackening hair The invention provides a composition for nourishing and blackening hair, which comprises 5 to 40 percent of snow lotus herb, 5 to 40 percent of red ant, 5 to 40 percent of raisin tree fruit and 50 to 80 percent of white spirit based on the total weight of the composition. After being preserved for 3 months at normal temperature, the composition is orally taken twice every day, 50 grams of composition is taken every time after a meal, and obvious effect can be achieved after one month. If the juice is coated on the hair and the hair is not washed in 4 hours till the hair is naturally dried in the air, the effect is better. The juice is squeezed liquid after aloe, white granulated sugar and the like are mixed in a weight ratio. After the juice is externally coated, ginger and hot pepper can be mashed to form juice which is uniformly coated on the scalp. The composition has remarkable effect.
US7005425 Administering a minimal dose of an Al adenosine receptor agonist in conjunction with a minimal dose of a beta blocker, calcium channel blocker, or cardiac glycoside Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A1 adenosine receptor agonist with a therapeutically effective minimal dose of a beta blocker, calcium channel blocker, or a cardiac glycoside.
WO2010148314A2 Preparation of esomeprazole and its pharmaceutically acceptable salts Processes for the preparation of esomeprazole and its pharmaceutically acceptable salts.
US20070270358 Cosmetic and/or Pharmaceutical Composition for the Treatment of the Rosacea The invention concerns a cosmetic, pharmaceutical, or medical device composition based on dimethyl sulfone to be applied on the skin, both integral and damaged, for the treatment of rosacea, acne, psoriasis, atopic dermatitis, dermatitis seborrheica, erythema intending by erythema also cutaneous flushing as it is called in the cosmetics field. The invention concerns also the use of dimethyl sulfone in combination with substances having anti-bacterial and/or anti-biotic activity, and metronidazole, flavonoids, vitamins, cortisone agents, tacrolimus for said treatment.
WO2014145308A1 Compositions and methods for delivering therapeutic and imaging agents to the sinuses and middle ear The present invention features compositions and methods for targeted delivery of a therapeutic or imaging agent to a site accessible through the nose or mouth that may be difficult to effectively and efficiently treat otherwise (e.g., the middle ear, sinuses, or lung). The therapeutic or imaging agent is deposited onto a magnetic nanoparticle that is drawn through a passage or tissue that leads away from the nose or mouth by a magnetic field applied over the targeted site (e.g., by magnets within the ear canal or surrounding the ear).
CN102370656A Clarithromycin medicine composition and preparation method thereof The invention discloses a clarithromycin medicine composition and a preparation method thereof; the dissolution rate of the clarithromycin in the water is increased and the absorption of the clarithromycin in the body is also increased; the specific technical scheme is as follows: in the clarithromycin medicine composition, the clarithromycin is used as the medicine active component; and the auxiliary materials are a filler, a disintegrating agent, a flavoring agent and a lubricating agent according to a weight ratio of 1-45:30-50:2.5-12:1-2.8:0.1-1. The method for preparing the clarithromycin medicine composition comprises the following steps of: (1) dissolving; (2) screening; (3) drying; and (4) tabletting. By using the clarithromycin medicine composition prepared according to the invention, the dissolution rate of the product can be increased and stable blood concentration can be maintained so that the medicine taking frequency can be reduced and the medicine taking interval can be prolonged.
WO2006053323B1 Inhibitors of hiv-1 capsid formation: substituted aryl aminomethyl thiazole ureas and analogues thereof Substituted aryl aminomethyl thiazole ureas and analogues thereof that act as inhibitors of viral capsid formation, including HIV capsid formation, are provided here. Generally the virus capsid formation inhibitors described herein are compounds of Formula (I) where A is a group of formula (a) or (b) wherein the variables A, R1, R2, R3, R4, X, Y, Z, A5, A6, A7, R8, R9, R12, and R13 are defined herein. Pharmaceutical compositions comprising such compounds and methods of treating animals infected with a virus having a capsid protein are provided herein. Methods of using such compounds to treat human patients infected with an HIV virus and reducing the mortality of AIDS are also provided herein.
CN103432144A Application of withanolide compound in preparation of drug or healthcare product for treating or preventing tumors and neurodegenerative diseases The invention discloses application of a withanolide compound in preparation of a drug or a healthcare product for treating or preventing tumors and neurodegenerative diseases. The withanolide compound has structural formulas as shown in formula I and optical isomers thereof. The research indicates that the withanolide compounds can be used for activating an Nrf2 signal channel, up regulating expression of NrF2 and downstream antioxidant and II-phase detoxifying enzymes thereof, strengthening the level of glutathione in cells, increasing reducing capacity in cells, promoting elimination of active carbon, restraining lipid peroxidation and lowering cytotoxicity caused by cancerogen arsenic and nerve cell toxicity induced by active oxygen H2O2 to show good chemical prevention effect. And therefore, the withanolide compound and nightshade extract including the withanolide compound have the potential of becoming a chemical prophylactic drug and the healthcare product, and can be used for preparing the corresponding oral preparation and injection by being used as the main ingredient, and also can be used for preventing and treating tumors and neurodegenerative diseases.
WO2013026025A1 Cyclohexyl azetidine derivatives as jak inhibitors The present invention provides cyclohexyl azetidine derivatives of formula (I), as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
US20090182054 Topical compositions containing solubilized dicarboxylic acids Topical compositions containing at least one solubilized dicarboxylic acid having 6 to 12 carbon atoms are prepared in pharmaceutically acceptable carriers in the presence of at least one 1,2-alkanediol having 5 to 7 carbon atoms. In particular, a topical composition containing solubilized azelaic acid is formulated in an aqueous carrier. In-vitro skin penetration and bioavailability study demonstrates higher bioavailability of the solubilized azelaic acid in the cutaneous organs. The topical composition is advantageous in treatment of skin disorders associated with skin inflammation such as rosacea, seborrheic dermatitis, perioral dermatitis, and facial dermatitis.
CA2341991C Pyrroloindoles, pyridoindoles and azepinoindoles as 5-ht2c agonists A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.
US20110038806 Medicaments for inhalation comprising an anticholinergic and a steroid A pharmaceutical composition comprising a compound of formula 1 wherein X− is an anion with a single negative charge, and a betamimetic, optionally together with a pharmaceutically acceptable excipient, the compound of formula 1 and the betamimetic optionally in the form of their enantiomers, mixtures of their enantiomers, their racemates, their solvates, or their hydrates, processes for preparing them, and their use in the treatment of respiratory tract diseases.
CA2432126C Complex of modafinil and cyclodextrin Mixtures of a modafinil compound with a cyclodextrin, methods for their use, and compositions thereof are disclosed, along with complexes comprising a modafinil compound and a cyclodextrin which are teste-masked and suitable for oral consumption in an aqueous solution.
CN102048703A Gatifloxacin dispersible tablets and preparation method thereof The invention discloses gatifloxacin dispersible tablets and a preparation method thereof. The dispersible tablets are prepared from the following raw materials and auxiliary materials in part by weight: 200 to 260 parts of gatifloxacin, 40 to 50 parts of crospovidone, 140 to 180 parts of microcrystalline cellulose, 30 to 40 parts of hydroxy propyl cellulose, 7 to 10 parts of stevia, 4.5 to 8 parts of magnesium stearate, and a proper amount of ethanol solution of povidoneK30; and the preparation method comprises the following steps of: taking the gatifloxacin, the microcrystalline cellulose, the hydroxy propyl cellulose, the stevia and the crospovidone according to the weight part ratio, respectively sieving by using a 80-mesh sieve, sieving by using a 60-mesh sieve, uniformly mixing, and preparing into a soft material by using the 4 percent ethanol solution of povidoneK30; sieving by using a 30-mesh sieve for granulation, performing forced air drying at the temperature of between 55 and 60 DEG C, and finishing the dry granules by using a 24-mesh sieve; and adding the crospovidone and the magnesium stearate according to the prescription, mixing, and tabletting. The tablets provided by the invention have good disintegration effect; and the granules prepared by the method have high fluidity and compressibility.
CN102731519A P-nitro aryl methoxycamptothecine anoxic activated prodrug used for antitumor drug The invention relates to an p-nitro aryl methoxycamptothecine anoxic activated prodrug used for an antitumor drug, its chemical name is (4S)-4,11-diethyl-4-hydroxy-9-(4-nitro aryl methoxy)-1H-pyrano [3',4': 6, 7]-indolizino[1,2-b) quinoline-3,14(4H,12H)-dione; by using an p-nitro aryl methylated modifier, under the alkaline condition, a reaction is carried out with SN-38 for p-nitro aryl methylation to prepare the p-nitro aryl methoxycamptothecine anoxic activated prodrug used for the antitumor drug-p-nitro aryl methoxy SN-38. The predrug can be used as a main effective component to prepare the antitumor drug, especially for the preparation of antitumor agents for treating colon cancer.
US7235247 Aqueous solution; efficient penetration The present invention provides a pharmaceutical composition for application to the mucosa to be used in drug therapy comprising a water-insoluble and/or water-low soluble substance, a medicament, and an aqueous medium, and having an osmotic pressure of less than 290 mOsm. This composition is superior over conventional pharmaceutical compositions for application to the mucosa, due to efficient and high permeability to the blood at the mucosa. The present invention further provides a pharmaceutical composition for application to the mucosa comprising a hemostatic agent and a medicament. This composition is superior over conventional pharmaceutical compositions for application to the mucosa, due to permeability and retentivity at the mucosa.
CN102898542A Water-soluble fullerene and application thereof The invention relates to a water-soluble fullerene and an application thereof; and problems that the traditional tumor therapeutic drug has a large side effect and cannot very well suppress tumor cell proliferation can be effectively solved; and a technical scheme for solving the problems is as follows: on the basis that the original fullerene is purified, the purified fullerene reacts with an ammoniation reagent; and after an amino with stronger reaction activity is connected to the surface of the fullerene, the fullerene reacts with a hyaluronic acid, so as to generate fullerene-hyaluronic acid polymer, wherein the mass ratio of the hyaluronic acid and the fullerene is 0.18-0.25:1; and the water-soluble fullerene provided by the invention has the advantages of good physical and chemical stability, easiness for satisfying preparation conditions, rich raw material sources, low cost and small side effect and is an innovation on a tumor therapeutic drug carrier.
CN102000067A Application of osthole in preparation of medicament for preventing and treating pulmonary fibrosis The invention relates to application of osthole in the preparation of a medicament for preventing and treating pulmonary fibrosis. A pulmonary fibrosis animal model of a rat is replicated through dripping BLM (Bleomycin) into an air tube; the osthole is selected as a treatment medicament for the first time to research the influence of the osthole on lung tissues and serum-related biochemical indicators and pathological variations of the pulmonary fibrosis rat, and the treating effect of the osthole on the pulmonary fibrosis rat model is observed, therefore, experiment basis is provided for pulmonary fibrosis preventing and treating effects of the osthol.
CN102949370A Roflumilast tablets as well as preparation method and detection method thereof The invention provides roflumilaste tablets as well as a preparation method and a detection method thereof. The roflumilaste tables are prepared by adopting 0.5mg roflumilast as crude drugs, adding 100mg to 150mg of lactose, 80mg to 120mg of pregelatinized starch, 10mg to 30mg of povidone K30 and 0.5 to 2.6mg of magnesium stearate and adopting acetone, ethanol and pure water as solvent. Aiming at the weaknesses of the prior art, the formula and the preparation process of the roflumilast tablets are optimized, so that a remarkable effect for treating diseases such as chronic obstructive pulmonary disease (COPD) is obtained, a systematic, complete and valid component discrimination and content determination method is established, the quality of the medicine can be effectively controlled, and the clinical effect of the roflumilast tablets can be guaranteed.
US20100239694 compositions of Acai fruit and Jucara fruit with high antioxidant capability and cyclooxygenase-inhibitory activity, and their uses The present invention relates to stable, palatable, freeze-dried, fruit-based compositions. Specifically, the inventions relates to compositions of Açai fruit and Jucara fruit with high antioxidant capability and cyclooxygenase-inhibitory activity, and their uses. The invention further provides for methods of making stable, palatable, freeze-dried, fruit-based compositions from Açai fruit and Jucara fruit.
US7205386 Truncated CD200 A truncated form of the full-length, immunosuppression-inducing molecule, CD200, CD200tr, was expressed in CHO cells and the transduced cells used to produce mAbs to CD200tr. These mAbs detect simultaneous expression of full-length CD200 and CD200tr in LPS-stimulated dendritic cells (DCs). Moreover, CHO cells and DCs expressing CD200tr as well as soluble CD200tr are able to inhibit suppression of mixed leucocyte reactions in vitro which follows addition of the soluble form of CD200 (CD200:Fc) in culture, demonstrating that CD200tr is a physiological antagonist of CD200.
WO2012047907A9 Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
WO2013105058A1 7,8- dihydropyrido [3, 4 - b] pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Formula (I)
CN103610653A Preparation method of netilmicin sulfate freeze-dried powder for injection The invention provides a preparation method of netilmicin sulfate freeze-dried powder for injection. The quality of the obtained netilmicin sulfate freeze-dried powder is greatly improved through the adjustment of process steps such as the adjustment of medicine adding sequences as well as the precise control over temperatures, time, pressures and other parameters, the multilayer control of filtration and the like. Thus, the storage life of the netilmicin sulfate freeze-dried powder is prolonged; the process is more normalized. As a result, the preparation method is suitable for being popularized.
EP2291351A1 Alpha-mercapto-amides Substituted amides of the general formula (I): with the residues A, R1 and R2 as explained in detail in the description are described. The compounds are suitable in particular as neutral endopeptidase inhibitors and are highly potent.
US20080176889 4-{2-[Bis-(2-chloroethyl)amino]ethoxy}-10H-acridine-9-one; Anticancer agents This invention relates to 9-anilinoacridine alkylating agents, their synthesis and their use in pharmaceutical compositions for treating diseases.
CA2378243C Methods for treating or preventing pain and anxiety The present invention relates to a novel method of treating of pain or anxiety, using compounds that modulate KCNQ potassium channels and currents.
US20080318910 Controlled-Release Oral Dosage Form A controlled-release oral dosage form suitable for administration to a mammal. The dosage form comprises a drug and an organic acid or a salt thereof. The dosage form releases no more than 60% the total amount of the drug within about a first hour, the remaining amount of the drug being released over a period of time of about 5 to about 8 hours subsequent to the first hour. Such a dosage form can be particularly useful for delivery of various pH-dependent solubility drugs.
EP1694318B1 (s)-2-n-propylamino-5-hydroxytetralin as a d3-agonist The invention relates to a medicament containing (S)-2-N-propylamino-5-hydroxytetralin, the salts or prodrugs thereof. As a D3 agonist, (S)-2-N-propylamino-5-hydroxytetralin is suitable particularly for the treatment of dopa-sensitive movement disorders.
WO2006040558A1 Substituted adenines and the use thereof This invention relates to compounds of Formula (I): and their use in the treatment of bacterial infections.
CN102091063A Application of furanodienone in preparing antipyretic medicament The invention provides an application of furanodienone in preparing an antipyretic medicament.
EP1934198B1 Polymorphs of benzoate salt of 2-[[6-[(3r)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2h)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor Compositions comprising Compound (I), wherein the Compound (I) is present in one or more polymorphic forms. Also provided are kits and articles of manufacture with compositions comprising one or more polymorphs of Compound (I), and methods of using the compositions to treat various diseases.
WO2012063896A1 Novel pyrazole amide derivative The present invention relates to a compound, said compound having excellent DGAT inhibitory effect and antifeeding effect, or a pharmacologically acceptable salt of the compound. A compound represented by general formula (I) or a pharmacologically acceptable salt thereof. In general formula (I): R1 represents a hydrogen atom, a halogen atom or a carboxyl group; R2 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, etc.; R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, etc.; T represents a nitrogen atom or a group represented by formula -CH=; W represents a nitrogen atom or a group represented by formula -CH=; U represents a nitrogen atom or a group represented by formula -CH=; V represents a nitrogen atom or a group represented by formula -CH=; Q represents a nitrogen atom or a group represented by formula -CH=; Z represents a nitrogen atom, a group represented by formula -CH= or a group represented by formula -C(R4)=; R4 represents a halogen atom, a C1-6 alkyl group, etc.; m represents 0 or 1; and n represents an integer of 0 to 2.
CA2554245A1 Novel hiv protease inhibitors The present invention provides novel HIV protease inhibitors containing substituted borane, carborane or metallacarborane clusters with 6 to 12 boron atoms in each cluster, wherein the charge of each borane, carborane or metallacarborane cluster is 0, -1 or -2; the number of borane, carborane or metallacarborane clusters in the inhibitor molecule is 1 to 9, and the carborane clusters in metallacarborane inhibitors are coordinated to transition metal atom, selected from the group containing cobalt, iron, nickel and ruthenium. In the cluster can be present heteroatoms as nitrogen, phosphorus, silicon, germanium, tin and sulphur. Pharmaceutical compositions containing these inhibitors and their use, both in vitro and in vivo. They are characterized by high effectivity and stability.
WO2009010794A1 2,4-diamino-pyrimidine derivatives The invention concerns compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, Q, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation ofsuch compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4 kinases.
US20100279994 Ansamycin Formulations and Methods of Use Thereof The present invention provides pharmaceutical compositions of reduced forms of benzoquinone-containing ansamycins, and salts thereof. The present invention also relates to the use of said pharmaceutical compositions in methods of treating and modulating disorders associated with hyperproliferation, such as cancer.
CN101757605A Medicine for preventing fish bacterial enteritis The invention discloses medicine for preventing fish bacterial enteritis, and relates to the field of aquaculture, in particular to Chinese and western compound medicine for preventing fish diseases. The medicine comprises the following components by weight parts: 10 to 20 parts of colistin sulfate, 30 to 50 parts of rhubarb, 40 to 60 parts of radix isatidis and 10 to 20 parts of garlicin. The medicine of the invention adopts a Chinese and western compound prescription, overcomes the problems that the fish suffers from bacterial enteritis in high-temperature seasons and the bacterial enteritis is easy to reoccur, has very good treatment effect to inflammatory bowel diseases caused by aeromonas hydrophila and other bacteria, and is characterized by significant therapic effect and no any toxic and side effect.
CN1883494A Solid-state molecular dispersible preparation of pennogenin compound The present invention relates to a special preparation form using pennogenin composite as an active constituent. Said pennogenin composite solid molecule dispersing preparation is formed by the mass percent of 0.5 to 40% pennogenin composite and 60 to 99.5% cyclodextrin. Composites with molecular weight over 1000 are generally supposed to be hard buried by cyclodextrin due to their big molecular space volume. The present invention is characterized in burying the pennogenin composite in cyclodextrin in a dispersing state in single molecule with the dispersing degree over ten times smaller than that of nanometer grains, which is quickly disintegrated and dispersed and absorbed by human body after entering into gastrointestinal tract, which as a result, improves the biological utility ratio by over two times. And the invention is also characterized in overcoming the shortcoming of PEG solid dispersant easily aging which results in slow dissolving-out speed. The present preparation is mainly used to cure gynecological blood diseases including hemostasis, hematopoiesis and gynecological inflammation.
WO2012145981A1 Adamantane or adamantane-like compounds as antitumor agents Chain compounds containing Adamantane or adamantane-like group, its stereoisomers, prodrugs, pharmaceutical salts, complex salt and solvate are provided. It comprises formula (I), where in S is a optionally substituted cyclic group, P is a optionally substituted functional group linkable S or T, T is a optionally substituted Adamantane or adamantane-like group, the structures of S, P, T can be combined all together or two kinds of them independently. The compounds have antitumor, antiviral, treating nervous system disease and inflammatory disease activities, and they can be used as drugs. Further, the present invention provides the preparation method for the compounds and use of the compounds.
EP0984969B1 Fused dihydropyrans Compounds of formula (I) in which the substituents have the meanings mentioned in the description, are suitable for the prevention and treatment of gastrointestinal diseases.
WO2012000933A1 3-amino-5,6-dihydro-1h-pyrazin-2-one derivatives useful for the treatement of alzheimer's disease and other forms of dementia The present invention relates to novel 3-amino-5,6-dihydro-1H-pyrazin-2-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta- amyloid.
US20120269907 Dialysis Machine Control A method of preparing a dialysate solution for hemodialysis, the method including the steps of providing a mixing pump comprising a pump chamber covered by an actuable membrane, the chamber having a first inlet for admitting water into the chamber, a second inlet for admitting dialysate base solution into the chamber, and an outlet from the chamber, the method including the further steps of providing pump means for dispensing a predetermined volume of dialysate solution base into the chamber at a first pressure, actuating the membrane to draw a volume of water or water mix into the mixing pump chamber at a second pressure, wherein the magnitude of the first pressure is higher than the magnitude of the second pressure so as to ensure the complete dispense of the dialysate solution base into the chamber.
US7771931 Using presence of allelic mutation in protein kinase c gene as diagnostic indication of heart disease The invention provides methods of diagnosing diseases and conditions associated with PKCλ, methods for identifying compounds that can be used to treat or to prevent such diseases and conditions, and methods of using these compounds to treat or to prevent such diseases and conditions. Also provided in the invention are animal model systems that can be used in screening methods.
CN103006755A Beggarweed extractive and general flavone and rhizoma kaempferiae glycosides separated from the beggarweed extractive and medical application thereof The invention relates to the field of medical technology, in particular to the application of desmodium podocarpum DC extractive and general flavone and rhizoma kaempferiae glycosides monomeric compound separated from the desmodium podocarpum DC extractive in preparation of medicine or food for preventing and curing osteoporosis. The desmodium podocarpum DC dried herb is taken as the raw material for extraction and separation so as to obtain the desmodium podocarpum DC extractive, and the desmodium podocarpum DC extractive is used for preparing general flavone of the desmodium podocarpum DC and the rhizoma kaempferiae glycosides monomeric compound is separated from the desmodium podocarpum DC. In vitro and vivo experiments show that the desmodium podocarpum DC extractive and the general flavone or the rhizoma kaempferiae glycosides monomeric compound of the desmodium podocarpum DC have good biological activity in anti-osteoporosis, thus being used for preparing medicine or food for preventing and curing osteoporosis. The preparation method is simple, and provides new medicine source for anti-osteoporosis.
US20060177444 Concomitant drug as therapeutic agent for inflammatory bowel disease An object of the present invention is to provide a medicament efficacious for an inflammatory bowel disease such as ulcerative colitis or Crohn's disease. Specifically, it provides a therapeutic agent for inflammatory bowel diseases comprising active ingredient (a) consisting of at least one compound having inflammatory inhibiting activity selected from the group consisting of an aminosalicylic acid derivative, an antiinflammatory glucocorticoid, an immunosuppressive compound, an anti-TNFα antibody, a neurohypophysial hormone and an antiinfective compound, combined with active ingredient (b) consisting of at least one compound having PPARγ agonistic activity, wherein the agent is so configured that the compound (a) and the compound (b) are used simultaneously, separately or every scheduled time.
CN102488746A Compound propolis composition for treating swine infectious atrophic rhinitis and preparation method thereof The invention relates to a compound propolis composition for treating swine infectious atrophic rhinitis and a preparation method thereof, which relates to the field of animal medicines. The preparation method for the composition comprises the following steps: (1) respectively carrying out ultrafine crushing on all the components in a prescription and screening all the crushed components with a 700-mesh sieve; (2) weighing 15 to 35 parts by weight of propolis, 15 to 35 parts by weight of fructus gleditsiae abnormalis, 15 to 35 parts by weight of dahurian angelica root and 15 to 35 parts by weight of Asarum herb and uniformly mixing the components for 5 to 10 min; (3) weighing 15 to 45 parts by weight of borneol, 10 to 20 parts by weight of realgar, 15 to 45 parts by weight of mint and 10 to 30 parts by weight of tarragon and uniformly mixing the components for 5 to 10 min; and (4) combining compositions prepared in step (2) and (3) and continuing to uniformly mix the compositions for 10 to 15 min so as to obtain the compound propolis composition. The beneficial effects of the invention are as follows: composition is reasonable; preparation is simple; the compound propolis composition has the advantages of no toxic and side effects, no pollution, no drug residue, no drug resistance, a unique application method of direct blowing of the compound propolis composition into noses of infected animals, ultrafine crushing, high bioavailability and a very remarkable curative effect, and according to results of clinical practice, the compound propolis composition has special efficacy in treating swine infectious atrophic rhinitis.
CN103550198A Medicinal preparation for treating constipation and preparation method thereof The invention relates to a suppository for treating constipation and a preparation method thereof. The suppository is characterized in that a matrix and a proper dispersant are added into docusate sodium and mixed to prepare rectal administration suppository. The suppository is controllable in quality, stable and mild in property, can be used for preventing and treating various constipations in different ages, is suitable for postoperative constipations of haemorrhoids, senility and weakness, cardiovascular and cerebrovascular diseases and in proctology, obstetrics and gynecology departments and the like, and has higher clinical application value for oral intolerance or special patients.
CA2656579A1 Novel tyrosinase inhibitors, their process of preparation and their use in human medicine and in cosmetics The present invention relates to the use of compounds corresponding to the following general formula (I) in pharmaceutical compositions intended for use in human or veterinary medicine or else in cosmetic compositions, and also to novel compounds of formula (II) and to the compositions comprising them.
CA2709396A1 Prevention of opportunistic infections in immune-compromised subjects This invention relates to a composition suitable for use in the prevention of opportunistic infections in immune-compromised individuals comprising a probiotic Bifidobacterium lactis, Bifidobacterium infantis, Bifidobacterium breve or Bifidobacterium longum and a fucosylated oligosaccharide selected from the group comprising 2'-fucosyllactose, 3'fucosyllactose, difucosyllactose, lacto-N- fucopentaose, lacto-N-fucohexaose, fucosyllacto-N-hexaose and fucosyllacto-N- neohexaose. The invention further extends to the use of such a composition in the prevention of opportunistic infections in immune-compromised individuals.
WO2009047336A1 Phthalazine and pyrido [3,4-d] pyridaz ine compounds as h1 receptor antagonists The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.
EP0752872B1 Nadh oxidase as a target in diagnosis and therapy Plasma membrane NADH oxidase is shown to be a target for a variety of uses in diagnotis and therapy. Particularly, the NADH oxidase associated with neoplastic cells is immunologically and biologically different from NADH oxidase associated with normal cells. Thus, the presence of tumor cells in patients can be monitored by monitoring serum or biopsy samples for the presence of disease associated NADH oxidase. By employing NADH oxidase as a target for inhibitors, tumor cells, virally infected cells and cells having multiple drug resistance may be specifically affected, while not affecting normal cells. Specific inhibitors having increased activity for disease associated NADH oxidase as compared to normal NADH oxidase are provided. The use of the NADH oxidase associated with tumor cells provides opportunities for assays for screening drugs that are specific for neoplastic cells and can serve as anticancer drugs or growth inhibitors.
EP1556054A1 Antagonizing nk1 receptors inhibits consumption of substances of abuse This invention pertains to the surprising discovery that administration of one or more NK1 receptor antagonists to a mammal can inhibit self-administration of a substance of abuse (e.g. alcohol). In one embodiment, this invention provides a method of inhibiting or reducing self-administration of a substance of abuse by a mammal. The method involves administering to the mammal an NK1 receptor antagonist in a concentration sufficient to reduce self-administration of a substance of abuse and/or craving for a substance of abuse (e.g. ethanol).
EP2129378B1 Therapeutic compositions comprising thromboserin or a salt thereof for use in the prevention or treatment of thrombosis in a patient at risk of bleeding There is provided the use of a 5-HT2A receptor antagonist to treat or prevent thrombosis, particularly arterial thrombosis, in a human or animal patient. The patient is suitably one who is at risk of bleeding, particularly those about to undergo, or those undergoing, surgery. A preferred 5-HT2A antagonist is thromboserin.
CN101264055A Cimetidine emulsion for treating esophagitis and gastropathy and preparation thereof The invention discloses a medicine for curing oesophagitis and stomach complaint, in particular to an antacid for curing oesophagitis, gastric ulcer, duodenal ulcer, stomachache, pyrosis, heartburn and acid regurgitation and a gastric mucosa protected medicine of cimetidine emulsion and a preparation method. The cimetidine emulsion for curing oesophagitis and stomach complaint is prepared with the following materials at a certain weight ratio, that is, cimetidine to soybean lecithin to soybean oil to poloxamer to glycerol is 5-15 to 6-18 to 70-120 to 5-15 to 18-50. The medicine for curing oesophagitis and stomach complaint has the advantages of low recurrence rate, simple formulation constituent, low dose, quick absorption and high bioavailability; the medicine also has the advantages of good curative effect, no side effect, low cost, good safety and reliability.
CN101791301A Application of diallyl disulphide in preparing broad-spectrum antiviral medicament The invention provides an application of diallyl disulphide C6H10S2 in preparing a broad-spectrum antiviral medicament for improving the immunity and regulation functions of the organism, in particular an application in preparing medicaments for treating influenza viruses of H1N1, H5N1, H7N7, H9N2, H3N2, H3N3 subtypes, RSV (Respiratory Syncytial Viruses), CVB3 (Coxsackie Viruses B3), ADV (Adenoviruses) and Clade 0, 1, 2.1, 2.2, 2.3 and 7 viruses.
EP2254861A1 The 1,3-disubstituted ureas, method of re aration and utilisation thereof The invention relates to 1,3-disubstituted ureas of general formula (I) where X is CH group or nitrogen, II1 is alkyl carbonyl, carbonyl or carbamoyl, and R2 is di fferent substituted phenyl, pyridyl. pyrazyl, pyrimidyl, quinolinyl and quinoxalinyl, and the method of preparing thereof which consist in treating aromatic amines with isocyanates in inert solvents at 20 to 12O0C. The obtained 1,3-disubstituted ureas are inhibitors of the activity of the acyl co¬ enzyme A: cholesterol acykransferase (ACAT) enzyme, and may be used to inhibit cholesterol esterification and absorption in hypercholesterolemia.
CN100998602A Application of chondroition sulfate for preparing medicine to relieve chronic pain An application of chondroitin sulfate in preparing the medicines for remitting chronic pain, especially the nervous chronic pain, is disclosed.
CA2157921C Pharmaceutical compositions comprising paracetamol and l-cysteine or a precursor thereof An improved process for the production of a pharmaceutical composition comprising p-hydroxyacetanilide and L-cysteine or a compound which is converted thereto in vivo comprises mixing p-hydroxyacetanilide and L-cysteine or its precursor in the solid state and then shaping the solid mixture.
CN102781441A Salts, solvates, and pharmaceutical compositions of macrocyclic ghrelin receptor agonists and methods of using the same The present invention provides novel salts and solvates of macrocyclic compounds that bind to and/or are functional agonists of the ghrelin (growth hormone secretagogue) receptor. The invention also relates to polymorphs of these salts and solvates, pharmaceutical compositions containing these salts or solvates, and methods of using the pharmaceutical compositions. These pharmaceutical compositions are useful as therapeutics for a range of disease indications, in particular, for treatment and prevention of gastrointestinal disorders including, but not limited to, postoperative ileus, gastroparesis, including diabetic and postsurgical gastroparesis, opioid bowel dysfunction, chronic intestinal pseudo-obstruction, short bowel syndrome, functional gastrointestinal disorders and gastrointestinal dysmotility, such as that occurring in conjunction with other disease states, in critical care situations or as a result of treatment with pharmaceutical agents. Additionally, the pharmaceutical compositions have application to the treatment and prevention of metabolic and/or endocrine disorders, cardiovascular disorders, central nervous system disorders, bone disorders, inflammatory disorders, hyperproliferative disorders, disorders characterized by apoptosis and genetic disorders.
WO2012033266A1 Novel artemisinin or deoxoartemisinin-glycolipid hybrid derivatives and antiangiogenic use thereof The present invention relates to a novel artemisinin or deoxoartemisinin-glycolipid hybrid derivatives and antiangiogenic use thereof. The artemisinin or deoxoartemisinin-glycolipid hybrid derivatives of the present invention exhibit two or more times stronger activity than the existing drugs and little or no cellular toxicity to address safety to human body.
CN1923190A Curcumenol intralipid for injecta and its preparation process The invention relates to a curcumenol intralipid used in injection and relative production. Wherein, it uses curcumenol intralipid and emulsion, etc to be mixed, sheared, and emulsified, to prepare the injection curcumenol intralipid. The invention is white liquid, with light, and the amount of curcumenol is 0.1-100mg/ml, its average diameter is 100-500nm, pH is 4.0-9.0. The invention has hihg efficiency without side effect, with better stability and solution.
CA2705370A1 Heteroaryloxy quinazoline derivatives Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.;R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
US20100317738 Compositions and methods for treating conditions associated with neuronal dysfunction The present invention relates to compositions and methods for the treating and empirically investigating conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity). In particular, the present invention provides compositions and methods for using flufenamic acid in the treatment and empirical investigation of conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity).
CN101810604A Spray taking salbutamol and ambroxol as active ingredients The invention relates to a spray taking salbutamol and ambroxol as active ingredients, which is prepared from salbutamol and ambroxol or salts thereof, or purified hydrates thereof serving as medicinal active ingredients and pharmaceutically acceptable auxiliary materials. The spray is prepared and developed by adding some specific types of auxiliary materials in certain proportions into the salbutamol and ambroxol or the salts thereof, or the purified hydrates thereof serving as raw materials according to the technological measure stated by the invention.
CN103059013A New crystal of Dasatinib monohydrate and preparation method thereof The invention relates to the technical field of medicines, in particular to a crystal III of Dasatinib monohydrate, its preparation method and pharmaceutical composition. The crystal III of Dasatinib monohydrate provided in the invention is very stable under the conditions of illumination, high temperature, high humidity and accelerated testing. The pharmaceutical composition of crystal III of Dasatinib monohydrate has good dissolubility, and can be stable under high temperature conditions. In addition, compared with prior art, the preparation method provided in the invention has the advantages of simple operation and controllable quality.
US20060122176 such as 5-(1,3-benzodioxol-5-ylmethylene)-1,3-thiazolidine-2,4-dione, used for the treatment and/or prophylaxis of autoimmune, cardiovascular or neurodegenerative disorders, inflammatory or kidney diseases, bacterial or viral infections, platelet aggregation, cancer, transplant rejection or lung injuries The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1, R2 and n are as described in the description.
CA2409845C Active substance combination containing a compound with an opioid effect and at least one further compound of formula i The invention relates to an active substance combination that contains a compound with an opioid effect and at least one further compound of the general formula (I) and/or one of its diastereomers and/or one of its enantiomers and/or at least one corresponding physiologically acceptable salt thereof. The invention further relates to medicaments that contain the inventive active substance combination, to pharmaceutical formulations that contain the active substance combination and to the use of the active substance combination for producing a medicament.
EP2307410A1 Aza-beta-carbolines and methods of using same Provided are compounds having the general structure according to Formula (I). Further provided are pharmaceutical compositions comprising these compounds. The invention still further provides methods of treating alcoholism, methods of reducing alcohol intake, methods of treating anhedonia, and methods of treating anxiety using theses compounds or the compositions containing them.
US6951858 Substituted 1,2,4-triazine-3,5-diones; male and female sex hormone related conditions GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1, R2, R3a, R3b, R4, R5, and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
CN101422581A Compound granular formulation for treating cervical spondylosis or complicated lumbar disease The invention relates to a compound granule preparation treating cervical spondylosis or complicated lumbar vertebra disease, and the prescription consists of material food, such as radix puerariae, cimicifuga foetida, notopterygium root, qianghuang, radix sileris, herba schizonepetae, lediaozhu, pepper roots, wild pearl barley roots, angelica dahurica, medicated leaven, myrrh, frankincense, pyritum, ground beeltle, notoginseng root, earthworm, bombys batryticatus, blood of dragon, strychnos alkaloids, pearl powders, sticky rice, malt sugar juice adhesives and the like. The compound granule preparation has the advantages of rich raw materials, easy preparation and spilt charging of the compound granule preparation, convenient in sue, strong targeting and guiding force, good curative effect, having no toxic and side effects and total effective rate reaching 100 percent and the like. The invention fills in the gap of subject area that the compound granule preparation has the roles of extracting qi and lifting, regulating qi and elevating yang, inducing tendons and entering collaterals, suppressing yin and entering cord, promoting blood circulation by removing blood stasis, clearing and activating the channels and collaterals, driving wind and dispelling cold, dissolving dampness and detumescence, nourishing liver and reinforcing kidney, smoothing governor meridian for treating cervical spondylosis, spondylopathy, or cervical spondylosis complicated lumbar vertebra disease syndrome.
US20050209286 RXR activating molecules Disclosed are molecules that activate an RXR receptor, wherein the molecule comprises an RXR binding portion which binds the RXR receptor and comprises a side pocket contacting residue which contacts a side-pocket 1 of an RXR receptor.
CN102755310A Composition drug preparation containing levodopa The invention relates to a solid oral extended-release preparation which provides extended-release levodopa and admantadine and can be tablets, capsules and micropills, and belongs to the technical field of drug extended-release preparations. The tablets, capsules and micropills can be ordinary gastric soluble or enteric soluble preparations; and the drug release form can be extended release or double release. The drug extended-release preparation which is composed of levodopa (levodopa salt) and admantadine (admantadine salt) is used for treating parkinsonism and other movement-related symptoms, diseases or syndrom.
US20110311519 Methods of treatment of bone degenerative diseases Methods of reducing bone loss and treating degenerative bone diseases such as osteoporosis are disclosed. The methods comprise administration of an agent that inhibits signaling through the IL-17 pathway, such as an antibody or a quinazoline analogue such as halofuginone.
WO2014086099A1 Glucopyranosyl derivative, preparation method and medical use thereof The invention relates to a C-aryl substituted glucopyranosyl derivative as an inhibitor of sodium dependent glucose transporter (SGLTs), the preparation method and the medical use thereof, in particular the glucopyranosyl derivative shown as general formula (I) or pharmaceutically acceptable salts or all stereoisomers thereof, the preparation method or pharmaceutical compositions containing the derivative and the use for treating diabetes and related diseases, wherein the definition of each substituent in general formula (I) is the same as that in the description.
CN103655579A Medicinal compound composition of irbesartan and hydrochlorothiazide and preparation method thereof The invention discloses a compound composition of irbesartan and hydrochlorothiazide. The composition can be made into granules, capsules, tablets and coated tablets. By screening and adopting a specific adhesive, the dissolution rate of the active ingredient irbesartan can exceed 94%, and the dissolution rate of hydrochlorothiazide can exceed 96%; after the composition is placed for 10 days at a high temperature of 60 DEG C, the dissolution rates of the two active ingredients are basically kept unchanged; and therefore, the composition has good stability and can meet the needs of clinical medication.
CN102058557A Multicomponent sustained-release preparation and preparation method thereof The invention provides a multicomponent sustained-release preparation and a preparation method thereof. An isolation layer is arranged between a sustained-release part and a quick release part in the sustained-release preparation to effectively isolate the interaction of a sustained-release tablet core and an external quick release coat, the external quick release part is quickly released completely, the isolation layer is quickly dissolved when meeting an aqueous medium, and the release of the sustained-release tablet core is not influenced. The technology can be applied to compound sustained-release preparations as required.
US20130040924 Bridged polycyclic compound based compositions for the inhibition and amelioration of disease A pharmaceutically active agent, a pharmaceutically active agent carrier and method of use thereof are described. In some embodiments, a system may include a composition. The composition may include one or more bridged polycyclic compounds. At least one of the bridged polycyclic compounds may include at least two cyclic groups, and at least two pharmaceutically active agents may be associated with the bridged polycyclic compound. In some embodiments, a bridged polycyclic compound may be pharmaceutically active. In some embodiments, a bridged polycyclic compound may be function as a carrier for pharmaceutically active agents.
CN1966507A Benzopyran[4,3-b] indole compound, its preparation method and uses The invention discloses a kind of benzopyran-[4, 3-b] derivatives and their preparation method and applications. The compounds are prepared by carrying out a reaction of 4-hydroxy-3-aryl coumarin and substituted chain. It is proved by pharmacological test that the compounds can be used as selective estrogen receptor modulators in the treatment and prevention of osteoporosis and improvement of female menopause-related diseases.
EP2269600A1 Treatment of sleep disorders using eplivanserin in COPD patients The present invention relates to eplivanserin or pharmaceutically acceptable salts or esters thereof for use in a method for treating sleep disorders in patients displaying COPD and to an article of manufacture and package, containing eplivanserin for that use.
CN101401816B Method for preparing Calcium polycarbophil particle The invention provides a method for preparing a calcium polycarbophil particle which is easy to completely disintegrate. The calcium polycarbophil is added with a disintegrant and a bulking agent, and subjected to granulating, drying and finishing to obtain the calcium polycarbophil particle, wherein after the calcium polycarbophil is evenly mixed with the disintegrant and the bulking agent, is added with wetting liquid containing a surface active agent and is subjected to granulating, drying and finishing to obtain the calcium polycarbophil particle. According to the total weight of the calcium polycarbophil particle (dry particle), the content of the surface active agent is between 0.1 and 20 percent, the preferable content is between 0.3 and 15 percent, and the most preferable content is between 0.5 and 10 percent. The addition of the surface active agent can effectively accelerate the quick disintegration of a tablet in water and 0.1mol/L HCL solution.
CN103599240A Oral liquid for treating polycystic ovarian syndrome The invention discloses an oral liquid for treating polycystic ovarian syndrome. The oral liquid is prepared from the following raw materials in parts by weight: 25-30 parts of semen cuscutae, 20-25 parts of fluoritum, 15-20 parts of radix rehmanniae recen, 15-20 parts of herba lycopi, 15-20 parts of glossy privet fruit, 15-20 parts of eucommia ulmoides, 10-15 parts of Chinese magnoliavine fruit, 10-15 parts of rhizoma atractylodis macrocephalae, 10-15 parts of semen plantaginis, 5-10 parts of radix angelicae pubescentis, 5-10 parts of astragalus membranaceus, 5-10 parts of cistanche deserticola and 5-10 parts of lumbricus. The oral liquid has principle effects of tonifying the kidney and invigorating the spleen, reinforcing kidney and removing stasis, invigorating the blood circulation and clearing damp, and has excellent curative effect on a patient suffering from polycystic ovarian syndrome in the clinical situation.
CN103599126A New application of grifola frondosa fermentation exopolysaccharide fermentation liquid The invention provides a new application of grifola frondosa fermentation exopolysaccharide fermentation liquid, namely an application of grifola frondosa fermentation exopolysaccharide fermentation liquid in preparing a medicine for preventing viral diseases of poultry. Mass clinical studies prove that grifola frondosa fermentation exopolysaccharide has a good treatment effect on the viral diseases of poultry, and particularly can relieve the clinical symptoms caused by virus infection, reduce the death rate of the ill poultry and promote the ill poultry to recover eating; generally, the ill poultry is cured in 5-7 days, and the curative effect is obvious. Meanwhile, the invention further discloses a grifola frondosa fermentation exopolysaccharide fermentation process which is simple and has high efficiency, and the obtained fermentation liquid can be used as a medicine directly applied to the treatment and prevention of the viral diseases of poultry.
EP2569267A1 Improved methods for preparing squalene An improved method for preparing squalene from a squalene-containing composition, said method comprising the steps of (a) a purification distillation carried out at a temperature T1; (b) a denaturing distillation carried out at a temperature T2; wherein steps (a) and (b) may be performed in either order; T1 and T2 are sufficient to cause squalene to boil; T2 > T1 ; and T2 > 200°C.
US20130052270 Use of Gold Nanoclusters in Ameliorating Oxidate Stress and/or Aging Disclosed herein is the novel use of a gold nanocluser for ameliorating oxidative stress and/or aging of a cultured cell or a subject having an oxidative stress and/or aging condition mediated by a vascular factor. The gold nanocluster has a particle size ranging from about 0.1 to 20 nm, and preferably is dihydrolipoic acid (DHLA) coated gold nanocluster.
WO2011106650A2 Novel p53-mdm2/p53-mdm4 antagonists to treat proliferative disease High-resolution structural information delineates key interactions between MDM2 or MDM4 and heterocyclic compounds that bind to these proteins. These compounds are potent agonists of the p53-MDM2/p53-MDM4 complex.
CN102188445A Compound preparation of aminophylline, and preparation method thereof The invention relates to a compound preparation of aminophylline, and a preparation method thereof. The compound preparation is a double-layer tablet comprising a white layer and a brown layer, wherein a weight ratio of the white layer to the brown layer is (0.4 to 0.6) to 1. Compared with the prior arts, the double-layer compound tablet provided by the invention can exert fully asthma relieving effects belonging to aminophylline drugs, wherein the white layer is dissolved fast in stomach and the brown layer is dissolved slowly in stomach and intestine to produce lasting effects, and the white layer of the double-layer compound tablet contains aluminium hydroxide and chlorphenamine maleate, wherein aluminium hydroxide and chlorphenamine maleate can reduce effectively side-effects of aminophylline on gastrointestinal tract. The double-layer compound tablet has good stability and is suitable for a large scale production.
CN101928254B Benzotriazole derivatives and preparation method and use thereof The invention discloses benzotriazole derivatives, which are characterized by having the following general formula, wherein A=H or OCH3; R=H or OH or OCH3; and R'=H or OH or OCH3. The benzotriazole derivatives have higher antiproliferative activity on human oral epithelial cancer cells, lung cancer cells and gastric cancer cells. Therefore, the benzotriazole derivatives can be applied to preparing medicaments for resisting tumor cell proliferation. The invention discloses a preparation method for the benzotriazole derivatives.
US20100120736 Mineralocorticoid Receptor Antagonists Compounds of the formula (I) are provided having a steroid skeleton and substitution characteristics in the A and B rings of the steroid skeleton effective for mineralocorticoid receptor antagonism, and rings C and D of the steroid skeleton having substituents thereon according to formula (I), wherein R1 is —OH or ═O; R2 is (C1-3)alkyl or (C2-3)alkenyl; R3 is selected from formulas (IIa), (IIb), (IIc). These compounds are useful in the treatment of inter alia aldosteronism, hypokalemia, hypertension, congestive heart failure, heart fibrosis, renal failure and restenosis.
US20120039954 Method of treating insomnia A method of treating insomnia comprising administering to a subject a formulation including zaleplon, wherein the formulation is adapted to release the zaleplon after a lag time of at least about one hour after administration of the formulation, and during which substantially no drug substance is released; provide a time of peak plasma concentration of about 3 hours to about 6 hours after administration; provide an elimination half-life after the time of peak plasma concentration of about 0.5 hours to about 0.3 hours; and provide an area under the curve of about 70 ng·h/mL to about 90 ng·h/mL.
CN1803131A Anticancer diterpene analog compound intravenous injection formulation, and its preparation method and uses The invention relates to an Anticancer diterpene analog compound intravenous injection formulation, and its preparation method and uses, wherein the injection comprises medicinal composite dissolvent and anticancer effective dose of diterpenoids of formula I, the composite dissolvent includes molecule inclusion carrier Captisol or Ecapsin. The diterpenoids are used as guest molecules to be coated into the Captisol or Ecapsin carriers as the host molecules. The coated diterpenoids have increased dissolvability in water.
EP1100892B1 Use of prohibitin rna in treatment of cancer It has now been found that the introduction of single stranded oligonucleotides of DNA or RNA, particularly RNA transcribed from portions of wild type prohibitin 3'UTR, into tumors leads to arrested cell proliferation. Significant reduction in the size of primary tumors has been observed following direct administration of prohibitin 3'UTR RNA. Induction of systemic immunity, as evidenced by the disappearance of metastases as well as the lack of tumor growth in rechallenged animals following prohibitin RNA therapy, has been observed. Thus, wild type RNAs transcribed from portions of a prohibitin 3'UTR, or single stranded DNAs comprised of portions of a prohibitin 3'UTR, or synthetically-made oligonucleotides of the same sequences, can be directly administered as therapeutic agents against tumors.
US20110020315 Treatment of inflammatory illnesses with ace2 The present invention relates to ACE2 for the therapeutic treatment or prevention of inflammation.
CN101244053A Novel dispersed system with docetaxel as main component The invention relates to a dispersion system with docetaxel as main component for injection, comprising a surfactant, an assistant surfactant and a specified amount of oil for injection. The volume ratio of oil phase to the surfactant is greater than 3 percent as well as less than and equal to 33 percent. The volume ratio of the assistant surfactant to surfactant is greater than or equal to 12.5 percent and less than 167 percent.
US20090253754 Fast dissolving films and coatings for controlled release of flavors, active pharmaceutical ingredients, food substances, and nicotine A fast-dissolving film for use as a platform for the delivery of material to the oral cavity, comprising a film forming agent; a plasticizing agent; and a fast-dissolving, water-soluble agent; and methods for producing same.
CN103417698A External drug for treatment of impetigo The invention provides external drug for the treatment of impetigo. The external drug is made by mixing well, by weight, 25-35 parts of coptis root, 15-25 parts of phellodendron bark, 15-25 parts of rhizome of Chinese atractylode and 5-15 parts of dried alum, crushing to obtain 100-mesh fine powder, sterilizing, preparing with 120-200g of sesame oil to obtain paste. The external drug is applied to infected parts for use. The external drug has the effects of clearing heat and toxicity, clearing damp and killing insects, promoting granulation to heal up sore and diminishing swelling to expel stasis, is effective in treating impetigo, is low in cost and has no toxic and side effects.
CA2555741C Method of stimulating hair growth The present invention is directed to the discovery that (3S,4R)-3,4~- dihydro-4-(2,3-dihydro-2-methyl-3-oxopyridazin-6-yl)oxy-3-hydroxy-6-(3~-hydroxyphenyl)sulphonyl-2,2,3-trimethyl-2H-benzo[b]pyran may be used to promote hair growth and alleviate alopecia.
CN101104644A Preparation for polysaccharide selenite and application thereof Disclosed are a preparation method and the applications of a polysaccharide selenous acid ester, belonging to the polysaccharide selenide technical field. The invention is characterized in that the polysaccharide selenous acid ester is made essentially by reaction between polysaccharide or carbohydrate complex and selenide reagent which is selenium Oxyhalide or the compound contains the selenium Oxyhalide. Feeding molar ratio of the selenide reagent and hydroxyl groups in the polysaccharide is 1:0.1-20. The invention also comprises the applications of the polysaccharide selenous acid ester in preparing anticancer drug and ant-oxidation drug. The polysaccharide selenous acid ester is produced by the reaction between the selenium reagent and the hydroxyl groups in sugar units, but not by selenite radicals substituting sulfate groups of the polysaccharide sulfate. The yield and the quality of the product are both higher than that of the products produced by other methods, and the selenium content is much higher than that of the products produced by the present technique.
US20080025965 Methods and compositions for the treatment of diseases or conditions associated with increased C-reactive protein levels The invention features methods and compositions for reducing the serum C-reactive protein (CRP) level in a patient in need thereof, and for treating diseases and conditions associated with an increased serum CRP level. The invention also features methods and compositions for treating a patient diagnosed with, or at risk of developing, periodontal disease by administering a tricyclic compound or an analog thereof and/or a tetra-substituted pyrimidopyrimidine or an analog thereof. The invention also features methods and compositions for reducing the serum CRP level in a patient in need thereof, and for treating diseases and conditions associated with an increased serum CRP level.
WO2005079789A1 Combinatorial therapy with an acetylcholinesterase inhibitor and (3ar)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate The present invention relates to an improved method of treating, reducing or delaying cognitive impairments associated with the β-amyloid peptide, either in combination with treatment by cholinomimetic replacement therapy or as a prophylactic treatment.
CN102078332A In-vitro cultured calculus bovis containing preparation for treating common cold in children and preparation method thereof The invention provides an in-vitro cultured calculus bovis containing preparation for treating common cold in children. The preparation is particles prepared from 4 to 8 parts of in vitro cultured calculus bovis, 70 to 80parts of acetaminophen, 1 to 2 parts of chlorphenamine maleate, 20 to 25 parts of amantadine hydrochloride, and proper sucrose and essence. The in vitro cultured calculus bovis is used to replace calculus bovis artifactus, side effects of emesis and jaundice caused by excessive free bilirubin contained in the calculus bovis artifactus can be reduced; and the in-vitro cultured calculus bovis containing preparation is ground and stirred by using an equivalent increasing method so that the medicament components can be effectively dispersed to reduce the side effect caused by nonuniform degree of dispersion of the chlorphenamine maleate and the amantadine hydrochloride.
CN101143142A Silybin supersaturated self-emulsion composition and preparation method thereof The invention discloses a supersaturated self-emulsion combination of silibinin and the preparation method of the combination. The invention can effectively improve the biological utilization degree of the silibinin and improve the curative effect of the drug with low cost and simple technology. The supersaturated self-emulsion combination of silibinin consists of the silibinin, an oil phase, an emulsification, a coemulsifier and a stabilizer. The weight percentages of the raw material and the complementary materials are 1 percent to 20 percent of the silibinin, 5 percent to 40 percent of the oil phase, 10 percent to 90 percent of the emulsification, 1 percent to 20 percent of the coemulsifier and 0.5 percent to 10 percent of the stabilizer. The preparation method is that the silibinin, the oil phase, the emulsification and the coemulsifier are heated and synchronously mixed under 20 to 100 DEG C to completely dissolve the silibinin, and the stabilizer is added to be mixed uniformly, and the combination can be obtained. The supersaturated self-emulsion of silibinin of the invention can spontaneously form a micro-emulsion with the nanometer grade granular size when meeting the body fluid after arriving at the inside of body by injecting or orally taking, which can obviously improve the drug solubility and increase the drug stability and improve the biological utilization degree of the drug.
CN101313894A Freeze-dried injection of proton pump inhibitor The invention relates to a proton pump inhibitor frozen powder injection agent and a preparation method thereof. The proton pump inhibitor frozen powder injection agent prepared by the method can be taken as a medicine for treating gastric ulcer, duodenal ulcer, erosive gastroesophageal reflux disease, helicobacter pylori and Zollinger-Ellison Syndrome. The proton pump inhibitor frozen powder injection agent is prepared through taking a proton pump inhibitor as an active ingredient, adopting crystallized filtration, freezing and drying. The preparation process comprises the following steps of: adding water for injection and alkali to the proton pump inhibitor, stirring to dissolve and mix uniformly; performing the crystallized filtration; after measuring the content, adjusting pH value of filtrate; using the water for injection for fixing volume and a millipore filter with 0.22 mu m for filtration; filling, partially arranging corks, arranging in trays, freezing out, pressing the corks, taking out from boxes, rolling openings, checking quality and packaging. The prepared proton pump inhibitor frozen powder injection agent has excellent re-dissolving performance, is more stable when used together with transfusion in clinical use, can not separate out, and has better inspection result for visible foreign matters and insoluble particles.
EP1012281B1 Human leukocyte calcium activated potassium channel polypeptide A novel human leukocyte calcium activated potassium channel polypeptide is described which is expressed at a high level in activated T-cells. A full length cDNA which encodes the novel calcium activated potassium channel polypeptide is disclosed as well as the interior structural region and the amino acid residue sequence of the native biological molecule. Methods are provided to identify compounds that modulate the biological activity of a human leukocyte calcium-activated potassium channel.
CN101434524A 4-(4-hydroxy-3-methoxybenzene methylene) curcumin, preparation thereof and use in preparing anti-cancer medicament The invention relates to a synthetic antineoplastic, in particular to the synthesis of 4-(4-hydroxy-3-methoxyl benzylidene) curcumin and an application thereof. The compound is prepared by the condensation of curcumin and Knovenagel. The compound, 4-(4-hydroxy-3-methoxyl benzylidene) curcumin can obviously inhibit various tumour cells, especially for K562, B16, HepG2, SW480 and SH-SY5Y cells. Compared with Cur, the compound has a better proliferation inhibition effect on K562, B16, HepG2, SW480 and SH-SY5Y cells obviously, and half inhibition concentration of the compound is about 1/9 of that of Cur. The compound can obviously inhibit size and weight of B16 tumor in vivo.
CN1820751A Tirofiban powder injection and its preparing method The present invention relates to new preparation form of Tirofiban, especially Tirofiban powder for injection, as antiplatelet medicine and its preparation process. The powder for injection consists of Tirofiban as active component, freeze drying support agent and pH buffering agent. The present invention expands the administration range of Tirofiban and raises the clinical administration level of Tirofiban.
US20100286225 Diazeniumdiolate compounds, a process for their preparation and pharmaceutical compositions containing them. Compounds of formula (I): wherein: R1 represents a hydrogen atom or a —COOR group, R2 represents a group G or a linear or branched (C1-C6)alkyl group substituted by a group G, wherein G represents a —(CH2)n-A-(CH2)m—B—(CR4R5)p—(CH2)o-R6 group as defined in the description, R3 represents a hydrogen atom, an alkyl group or an NO2 group.
WO2010088455A2 Cromolyn derivatives and related methods of imaging and treatment Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula (I), or formula (II); wherein X is OH, C1-C6 alkoxyl, 18F, or 19F; Y and Z are independently selected from a C1-C6 alkyl, C1C6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H, X is not OH.
WO2012100654A1 Ribofuranosyl purine compound, preparation method therefor, and use thereof The present invention relates to compounds represented by General Formulas (I) and (I-1), and a preparation method therefor, a use of the compounds in treatment of platelet aggregation-related diseases and in preparation of drugs for treating platelet aggregation-related diseases, and a pharmaceutical composition and a pharmaceutical preparation containing the compounds, wherein in the general formulas, R1, R2, R3 and R2a have the same definitions as those in the specification.
WO2008100202A1 A 2-f luorobenzoate salt and a 2, 6-dif luorobenzoate salt of n-{5-chloro-2- [ ( (2s) -3-{ [1- (4-chlorobenzyl)piperidin-4- yl ] amino } - 2 - hydroxy- 2 -me t hylpr opyl ) oxy] - 4 - hydroxyphenyl } acetamide The invention provides a 2-fluorobenzoate salt and a 2,6-difluorobenzoate salt of N-{5-chloro-2-[((2S)-3-{[1-(4-chlorobenzyl)piperidin-4-yl]amino}-2-hydroxy-2-methylpropyl)oxy]-4-hydroxyphenyl}acetamide or a solvate and polymorhpic forms thereof, pharmaceutical compositions containing the salts or solvates and use thereof in therapy.
CN101513444A Medicine for treatment of aftosa The invention discloses a medicine for the treatment of aftosa, which is capable of playing roles of preventing and treating the aftosa and comprises live-spleen toxic dampness powder and live-spleen toxic dampness liquid, wherein, the live-spleen toxic dampness powder comprises (based on weight proportions): 8-12 parts of gypsum root, 6-8 parts of talcum, 3-5 parts of liquorice and 0.8-1.2 parts of ciliate desert-grass; the live-spleen toxic dampness liquid comprises (based on weight proportions): 18-22 parts of borax, 0.8-1.2 parts of ciliate desert-grass liquid, 7-12 parts of menthol and 1000 parts of boiling water.
EP1616564A2 Manipulation of nitrosative stress for treating microbes and helminths Manipulators of nitrosative stress are used to treat mammalian disease by selectively killing, or inhibiting the growth of, pathologic microbes or helminths or pathologically proliferating mammalian cells or by upregulating nitrosative stress defense mechanism. Novel agents include α-alkyl-S-alkyl-homocysteine sulfoximines wherein the α-alkyl contains 2 to 8 carbon atoms, and the S-alkyl-contains 1 to 10 carbon atoms.
WO2012139925A1 Labelled and un-labelled methyl-pyrrolyl-oxadiazolyl-diazabicyclononane derivatives and their medical use The present invention relates to certain labelled or un-labelled pyrrolyl-oxadizolyl-diazabicyclononane derivatives and their medical use. Furthermore, the present invention relates to the use of said derivatives in their labelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).
CN103450164A Geldanamycin derivatives as well as preparation methods and uses thereof The invention relates to novel geldanamycin derivatives, a preparation method of the geldanamycin derivatives, uses of the geldanamycin derivatives in the preparation of cell killers with cell killing activities, cell proliferation inhibitors and anti-tumor medicines, and uses of the geldanamycin derivatives in the preparation of biological probes for inhibiting the cell cycle. The invention also relates to medicine compositions comprising the geldanamycin derivatives provided by the invention. The geldanamycin derivatives provided by the invention can be used for treating diseases characterized by excessive cell proliferation, such as cancers.
CN101946985A Element fabric health-improving protective clothing capable of killing and repelling mosquitoes The invention relates to element fabric health-improving protective clothing capable of killing and repelling mosquitoes, which belongs to the technical field of the production of healthy textile multifunctional textile fabric clothing. More than 360 types of mosquitoes are recorded in China. The mosquitoes are fond of sucking blood of warm-blooded animals, infect malaria, filariasis, yellow fever, dengue, epidemic encephalitis B and even H1N1 flu and threaten human health. The element fabric health-improving protective clothing, which is produced by performing nanometered disposal on mixed materials of a plurality of trace elements needed by a human body, a broad-spectrum powerful silver antibacterial agent, an anti-mosquito finishing agent SCJ-951, mosquito-killing pyrethrin and the like and adding the mixture into spinning solution of cotton, flax, fur, polypropylene fiber, polyamide fiber, acrylic fiber and the like, kills and repels mosquitoes and improves health.
CN103211831A Application of flavone C-glycoside compound in preparation of COX-2 The invention discloses a flavone C-glycoside compound (I):, and an application of the flavone C-glycoside compound in preparation of a COX-2 inhibitor; wherein R1 is H, MeO or beta-D-glu; R2 is H, beta-D-glu or beta-D-glu-(2-1)-alpha-L-rha.
CN101418294A Antisense nucleic acid of methicillin-resistant staphylococcus aureus resistance gene mecA The invention relates to antisense oligodeoxynucleotide sequence aiming at a drug resistant gene mecA of a methicillin resistant staphylococcus aureus (MRSA), preparation for medicines containing the antisense oligodeoxynucleotide sequence, and application of the antisense oligodeoxynucleotide sequence. The antisense oligodeoxynucleotide sequence is characterized in that the antisense oligodeoxynucleotide sequence can be combined with different regions of the drug resistant gene mecA of the MRSA, and block the expression of the drug resistant gene mecA; the base sequence of the antisense oligodeoxynucleotide is PS-ODNs01-20; and the antisense oligodeoxynucleotide can be combined with a specific site of a target gene, so as to inhibit the expression of the drug resistant gene, restore the sensitivity of MRSA to beta-lactam antibiotics, and effectively resist the drug resistance of MRSA.
CN101585861B N-glycosyl naphthocarbazole compound and synthesis method and application thereof The invention belongs to the field of chemical synthesis, and relates to an N-glycosyl naphthocarbazole compound and synthesis method and application thereof for the preparation of antineoplastic medicaments. The N-glycosyl naphthocarbazole compound has the structural formula as shown in formula (I), wherein R<1> is D-glucosyl, L-rhamnosyl, D-ribopyranosyl, 2-deoxy-D-ribopyranosyl, D-ribofuranosyl, 2-deoxy-D-ribopyranosyl, D-galaetosyl, L-fucosyl, D-xylosyl, D-arabinosyl, L-arabinosyl, galaetosyl or maltosyl; R<2> is H, 2 or 4-substituted Cl, Br, F, OMe, OEt, CF3, or CH3; and R<3> is H, 8, 9,10 or 11-substituted Cl, F, Ome or OEt. As proved by experiments, the N-glycosyl naphthocarbazole compound has obvious inhibiting effects on breast cancer and pancreatic cancer cells; and the N-glycosyl naphthocarbazole compound is the selective inhibitory agent of D1/CDK4, has high inhibition activity, good water solubility and simple preparation and can be further prepared into antineoplastic medicaments.
US7700653 Hypotensive agents; cardiovascular disorders This invention relates to methods for treating cardiovascular disorders selected from heart failure, thromboembolic disorders, venous diseases, and fibriotic disorders other than fibrosis of the liver, comprising administering an effective amount of a compound of formula (I) wherein the several variables are as defined in the specification and claims.
CN103641818A Novel crystal form of tandospirone citrate, preparation method and applications The invention discloses a novel crystal form of tandospirone citrate, a preparation method for the novel crystal form and applications. The novel crystal form of tandospirone citrate can raise dissolvability and stability of original products, is beneficial for preparation and usage of the products and raises the product safety.
EP2266628A2 Method of determining the susceptibility to bone meatastases by EPhA2 expression The invention provides, inter alia, models of bone metastasis, methods for identifying agents that modulate skeletal related events and metastasis, methods for modulating skeletal related events and metastases, and methods for detecting skeletal related events and metastases. The methods and models generally comprise co-culturing cancer cells and host cells and comparing biological markers from such co-cultured cells to control cells.
CN102731442A Preparation method and application of water-soluble docetaxel compounds The invention discloses water-soluble docetaxel compounds, a medicine composite containing the water-soluble docetaxel compounds, as well as a preparation method and application of the water-soluble docetaxel compounds. The water-soluble docetaxel compounds are sodium salts or potassium salts of a multi-carboxyl compound I which has a structure shown in the specification. The preparation method of the water-soluble docetaxel compounds is simple, convenient and quick, high in yield and suitable for large-scale industrial production; and after docetaxel is modified by using the method, the chemical properties are stable, water solubility is improved greatly, toxicity is low, and the bioavailability and the antitumor effect are excellent.
CN101190935A Compound used for viral infect The invention pertains to the technical field of medicine, relating to new compounds, which have the activity of antivirus, etc., or stereoisomer and salt thereof, the preparation methods of the compounds or stereoisomer and salt thereof, medical compositions which comprise the compounds or stereoisomer and salt thereof as necessary active ingredients, and the application of the compounds or stereoisomer and salt thereof in the preparation of medicines to cure and/or prevent viral infection and hepatopathy. The compounds or stereoisomer thereof of the invention have prominent functions of antivirus, in particular to hepatitis B virus and human immunodeficiency virus, and have prominent activity to resist acute and chronic hepatic injury at the same time.
CN103750301A Flavour composition capable of enhancing immunity The invention relates to a flavour composition capable of enhancing immunity. The flavour composition contains arginine, a pulicaria insignis extract and seasoning base stock.
US20070036875 Use of allicin as preservative, as disinfectant, as antimicrobial or as biocidal agent The present invention provides the use of allicin in (i) the treatment of leishmaniasis; (ii) as a disinfectant or biocida treatment of aquatic species; (iii) as an antimicrobial agent for animal feed; (iv) as a preservative agent in foodstuffs; (v) as a water disinfectant or biocide; (vi) as an antiparasitic treatment or antibacterial treatment for bees (apis); or (vii) in the preparation of a medicament for the treatment of Glycopeptide Intermediate Resistant Stapohylococcus Aureus.
US20080242654 N-[(2Z)-3-butyl-4,5-dimethyl-1,3-thiazol-2(3H)-ylidene]-5-chloro-N',2-dimethoxybenzenecarboximidamide; CB2 receptors ligand; antiinflammatory, analgesic agent; autoimmune diseases; neuroprotectants The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, R4, L2 and A are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
CN103272068A Chinese and western medicine compound preparation containing tilmicosin and preparation method thereof The invention discloses a Chinese and western medicine compound preparation containing tilmicosin. The Chinese and western medicine compound preparation containing tilmicosin comprises the following components by mass percent: 2-30% of tilmicosin, 0.5-10% of taurine, 5-30% of milkvetch, 5-30% of isatis root, 5-30% of indigowoad leaf and the balance of officinal filling auxiliary material. The invention also discloses a preparation method of the Chinese and western medicine compound preparation containing tilmicosion. The Chinese and western medicine compound preparation containing tilmicosion has the advantages of stable effect, convenience in application and easiness in preparation when being used for treating respiratory diseases of beasts and birds.
CA2275167C The topical use of kappa opioid agonists to treat ocular pain Compositions and methods for treating ocular pain are disclosed. In particular, the invention discloses compositions and methods of using kappa opioid agonists topically for the prevention or alleviation of ocular pain.
WO2011060976A1 Tryptamine-derived compounds as antibacterial agents The present invention relates to a compound according to formula I, a pharmaceutically acceptable salt and/or N-oxide thereof for use as an antibacterial agent.
CN101522198B Pharmaceutical formulation for the treatment of complaints The present invention relates to a pharmaceutical formulation characterised in that it comprises mainly clobetasolpropionate, minoxidil, and 11 alpha-hydroxyprogesterone as active principles, as well The present invention relates to a pharmaceutical formulation characterised in that it comprises mainly clobetasolpropionate, minoxidil, and 11 alpha-hydroxyprogesterone as active principles, as wellas other excipients, vitamins and/or minerals, and it relates to the use of this formulation in the treatment of skin complaints, mainly in the symptomatic treatment of psoriasis.as other excipients, vitamins and/or minerals, and it relates to the use of this formulation in the treatment of skin complaints, mainly in the symptomatic treatment of psoriasis.
WO2003045918A8 Piperidine-based mch antagonists for treatment of obesity and cns disorders The present invention discloses compounds of formula I, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
CN101857613A Rupestonic acid glycolipid derivative and preparation method and applications thereof The invention relates to a rupestonic acid glycolipid derivative and a preparation method and application thereof. The derivative is prepared by synthetizing rupestonic acid and fully acetylized glycosyl bromide as raw materials under the action of tetraethyl benzyl ammonium chloride of a phase transfer catalyst, and a preliminary in vitro anti-influenza A (H3N2 and H1N1) and B virus activity test is carried out on the synthetized derivative. The test result shows that compounds 2d and 2g have better inhibitory action on the influenza A (H3N2) viruses, and by-products 3 have better inhibitory action on influenza A (H3N2 and H1N1) and B viruses. The method has mild reaction condition and simple and direct test steps.
US20090215900 Composition and method for providing glutamine A process for preparing a glutamine-supplemented food product by contacting water and a nutritive base that pre-dominantly comprises meat and carbohydrate with a peptide source of glutamine to form a wet mixture and heating the wet mixture at a temperature of from about 50° C. to about 105° C. for a time sufficient to cook the nutritive base. The process forms a cooked food composition comprising from about 60% to about 85% by weight water. The product is useful for feeding to an animal to increase glutamine absorption or to strengthen immune function.
CN101361848A Vaginitis treating medicine The invention relates to a medicine for curing gynecopathy, in particular to a medicine for curing vulvovaginitis. The technical proposal adopted by the invention is that: the medicine consists of components of the following weight ratio: 50g to 100g of radix sophorae flavescentis, 50g to 100g of rhizoma atractylodis, 5g to 8g of borneol, 10g to 15g of phellodendron, 20g to 40g of liquorice extract, 5g to 8g of sulphur, 20g to 40g of schisandra arisanensis, 2g to 8g of camphor and 20g to 40g of radix geutianae; all the components are fetched, dried and mixed evenly for preparing aerosol or suppository for external use. The medicine of the invention has the advantages of antisepticising, anti-inflammatory, relieving itching and being capable of curing the vaginitis thoroughly.
US20090018153 antiproliferative; cancer, psoriasis; increased bioavailability This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
US20110280832 Eotaxin-2 (ccl24) inhibitors in inflammatory, autoimmune, and cardiovascular disorders The presently described subject matter is based on the finding that inhibition of eotaxin-2 by polyclonal or monoclonal antibodies, has a significant protective effect in animal models of inflammatory diseases such as rheumatoid arthritis, experimental autoimmune encephalomyelitis (EAE), colitis, diabetes, and atherosclerosis. Thus, provided are pharmaceutical compositions including specific anti-eotaxin 2 antibodies for use alone or in combination with other therapeutic agents in the treatment of inflammatory, autoimmune and cardiovascular diseases. Also provided are specific anti-eotaxin-2 monoclonal antibodies, and methods of treatment utilizing such antibodies.
WO2013037065A1 Microrna inhibitors The present invention relates to microRNAs (miRNAs) that are associated with obesity. The present invention is directed to methods, compounds, and compositions for preventing and treating obesity, as well as related diseases, using a microRNA inhibitor.
US20120064130 Method for impregnation with supercritical co2 The present invention relates to a batch method for impregnating a nonporous polymer pharmaceutical carrier with an active substance, characterised in that said method includes the following consecutive steps: a) mixing the active substance and the nonporous polymer pharmaceutical carrier, the pharmaceutical carrier being in a solid form and insoluble in supercritical CO2 and not being non-crosslinked polyvinylpyrrolidone; b) performing a step of molecular diffusion in the absence of water by contacting, in a static mode without agitation, the mixture obtained in step a) with supercritical CO2 at a pressure of 80 to 170 bars, at a temperature of 31 to 90° C. for 1 to 6 hours; c) recovering the polymer pharmaceutical carrier impregnated with the active substance obtained in step b), the impregnated pharmaceutical carrier being nonporous and being in a solid form and the active substance being in an amorphous form, the method being implemented in the absence of an additional solvent. The invention further relates to a polymer pharmaceutical carrier in a nonporous solid form impregnated with an active substance characterised in that said carrier can be obtained by the method according to the present invention, in that the active substance is in an amorphous form and is water-soluble, and in that the polymer pharmaceutical carrier is not non-crosslinked polyvinylpyrrolidone and is insoluble in supercritical CO2.
US20080242718 point-of-care platelet analyzer device optimized for neuro-psychiatric analytes; testing and software predetermines risks of developing various neuropsychiatric conditions, like depression, Parkinson's, Alzheimer's, bipolar disorder, ADD/ADHD, autism, asperger's syndrome, OCD and other anxiety disorders The invention concerns in-vitro evaluation of intracellular biomarkers by doing blood testing. Concentrations of neurotransmitters in the platelet cells are utilized to identify chemical imbalance in the central nervous system. In one embodiment of the invention, testing data is analyzed by proprietary software algorithms by physicians and related health care professionals to diagnose and treat sufferers of chemical imbalance objectively. In another embodiment of the invention the testing and software predetermines risks of developing various neuropsychiatric conditions, like depression, Parkinson's, Alzheimer's, bipolar disorder, ADD/ADHD, autism, asperger's syndrome, OCD and other anxiety disorders, muscle disorders, etc.
CA2643633A1 The use of an antibody directed against beta amyloid peptide for the treatment of alzheimer's disease The invention provides preferred dosage ranges, maximum concentrations, average concentrations and monitoring regimes for use in treatment of Alzheimer's disease using antibodies to A.beta.. The invention also provides monitoring regimes that can assess changes in symptoms or signs of the patient following treatment.
WO2009154505A1 Membrane stabilising agent The invention relates to medicine and can be used in pharmacology as a preparation which exhibits non-specific membrane stabilising action. Iodine-antipyrine is claimed as a membrane stabilising agent. The found property makes it possible to use said agent for treating toxic liver injuries, hepatitis, oncological pathology (for complex treatment of oncological patients by radiotherapy and chemotherapy) and for many other pathologies caused by the toxic injury of an organism in its integrity and of the individual systems thereof.
CN101502511A Amoxicillin/clavulanate potassium tablet and preparation method thereof The invention provides an amoxicillin/clavulanate (8:1) tablet and a preparation method thereof. The amoxicillin/clavulanate (8:1) tablet has the advantages of simple preparation process, good quality controllability and stability and low forming-production cost by adopting the mixed amoxicillin/clavulanate (8:1) intermediate materials having good quality controllability and stability as the main drug resource.
US20080255064 Biological assay; experimental reporter expression vector has cholecystokinin promoter upregulating agent operably linked to experimental Renilla luciferase reporter gene; separately detectable; co-transform experimental vector and control vector in pancreatic islet host cells; increase plasma insulin The invention provides a method for upregulating cholecystokinin (CCK) expression in mammalian pancreatic islets by administrating a CCK upregulating agent. The increased CCK expression activates islet cell proliferation triggering an increase in pancreatic β-cell mass and plasma insulin levels. Accordingly, methods to produce a replenishable supply of islet cells and to ameliorate the symptoms associated with diabetes are also disclosed.
US7125564 Glycyrrhizin complex The products and methods of the present invention provide a means for increasing the solubility and bioavailability of active agents. More particularly the invention provides compositions containing active agents as water-soluble complexes with glycyrrhizin, and methods of preparing such complexes. The invention further provides methods for the preparation of highly water soluble complex dosage forms.
CN1634125A Health caring food for relieving constipation physically The invention discloses a health caring food for relieving constipation physically, which comprises the following raw materials (by weight portion), sodium alginate 10-80%, Kara gel 15-85%, fruity agent 5-30%. The health food has good action for improving the large intestine's defecating function.
US20080000473 pH-Based Methods and Devices for Preventing Hemagglutinin Cell Membrane Fusion The invention relates to devices and methods for treating or preventing avian flu, influenza and similar conditions using basic compounds, such as sodium bicarbonate, inhaled through inhalation devices such as nebulizers and the like. The invention also relates to processes for making the solution that is filled into the inhalation device. For example, the nebulizer can include a basic solution and at least a portion of the basic solution may be contained within one or both of a liposome and/or a micelle.
CA2678514A1 Chemical linkers with single amino acids and conjugates thereof The present disclosure provides drug-ligand conjugates that are potent cytotoxins and include a linker between the drug and ligand where the linker has a single amino acid. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.
US20100256091 Pharmaceutical powder compositions A powder composition for intranasal delivery includes a benzodiazepine drug and chitosan, a salt of chitosan, a derivative of chitosan or a salt of a derivative of chitosan.
US6946555 Preparation of triazoles by organometallic addition to ketones and intermediates therefor The invention provides a process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reaction of a compound of the formula: wherein R is as previously defined for a compound of the formula (I), with a compound of the formula: wherein R1 and “Het” are as previously defined for a compound of the formula (I) and X is chloro, bromo or iodo, in the presence of zinc, iodine and/or a Lewis acid and an aprotic organic solvent: said process being optionally followed by conversion of the compound of the formula (I) to an acid addition or base salt thereof.
WO2011061498A3 Inhalation solutions A inhaler for an inhalation formulation, comprising a canister containing a pharmaceutical composition under pressure; a metering valve for measuring a metered dose of the composition from the canister for administration to a patient in need thereof; and an actuator for actuating discharge of the metered dose to the patient; wherein the actuator includes a discharge orifice having a diameter in the range 0.2 to 0.4 mm; and wherein the pharmaceutical composition comprises an anticholinergic agent and a pharmaceutically acceptable propellant.
WO2009064486A3 Inhibitors of pim protein kinases, compositions, and methods for treating cancer The disclosure relates to inhibitors of Pim-1 and/or Pim-2 protein kinase, to compositions comprising one or more inhibitors of Pim-1 and/or Pim-2 protein kinase, and to methods for treating cancer.
CN101745088A Damp pain-relieving rubber paste and making method thereof The present invention provides a making method of a damp pain-relieving rubber paste with good performance. On the basis of the recipe of an original damp pain-relieving paste, the damp pain-relieving rubber paste is made of special hot melt polymer adjuvant matrix, wherein the special hot melt polymer adjuvant matrix is made of a hot plastic elastic body, medical rubber, softeners, antioxidant and the like which are prepared according to certain proportion. The making process of the damp pain-relieving rubber paste with good performance is simple, organic menstruum is not needed, and the making method of a damp pain-relieving rubber paste with good performance is safe and environmental. The rubber covering speed is fast, and the production efficiency is high. The damp pain-relieving rubber paste made by the present invention has small stimulation for skins, and has no allergic phenomenon. The sticking is comfortable. The damp pain-relieving rubber paste can not pollute clothes, can not stick hair, can be stuck repeatedly, and is the upgrading change generation product of damp pain-relieving paste plaster.
CN101474246B Pharmaceutical composition for enhancing immunity of fowl and coordinating with vaccine for synergy The invention discloses a pharmaceutical composition with the functions of enhancing the fowl immunity and matching vaccine to enhance the efficacy. The components and the weight percentage thereof are as follows: 0.5 to 5 percent of astragalus polyose, 0.5 to 5 percent of glycyrrhizin, 0.5 to 5 percent of icariine, 0.5 to 3 percent of propolis, 0.02 to 0.1 percent of vitamin E and addition agents. The pharmaceutical composition of the invention can obviously improve both the fowl body cellular immunity and the humoral immunity, and has favorable functions of preventing and controlling the immunosuppressive diseases of the fowl; second, the pharmaceutical composition can be matched with the vaccine to be used to improve the fowl antibody titer, thereby causing the antibodies to be comparatively uniform and to maintain a higher level and showing obvious functions of immunization and efficacy enhancement; and the pharmaceutical composition can be matched with medicines for curing the fowl newcastle disease, the bursa of fabricius, the bird flu and the like, thereby improving treatment effects, increasing the antibody guard time and reducing loss.
US20080102162 Prebiotic Preparation The present invention relates to a nutritional additive comprising arabinoxylans, which beneficially modulates the human intestinal flora. Furthermore, several food and beverage products comprising the additive are provided as well as methods to prepare the said additive.
CN102731530A Novel cephalosporin compound and its synthesis method and use The invention provides a novel cephalosporin compound. The novel cephalosporin compound has a general structural formula I, wherein in the general structural formula I, R1 represents nitrogen and sulfur heteroatom-containing five-membered heterocyclic radical or alkyl-substituted five-membered heterocyclic radical; R2 represents amino; and R3 represents C1-6 alkyl or organic acid ester-substituted alkyl. The invention also provides a synthesis method and a use of the novel cephalosporin compound having the general structural formula I. The novel cephalosporin compound having the general structural formula I has a certain activity of resisting standard staphylococcus aureus and standard klebsiella pneumoniae.
WO2011038924A9 Proteasome inhibitors for treating cancer A method is provided for treating cancer in a patient comprising administering to said patient a proteasome inhibitor at least three days a week.
WO2011075539A2 Treatment of obesity or diabetes with bile acid sequestrants Provided herein are methods of treating obesity and diabetes with labile bile acid sequestrants. An effective amount of a labile bile acid sequestrant may be orally administered to an obese or diabetic individual. A labile bile acid sequestrant provided herein may have a low affinity in the colon or rectum of a human for at least one bile acid or bile acid mimic that stimulates L-cells. A labile bile acid sequestrant may be a non-systemic labile bile acid sequestrant.
CN101554368A Tetrodotoxin composition formulation stable at room temperature and used for injection The invention relates to the production of medicament made of tetrodotoxin and derivative thereof, in particular to a stable tetrodotoxin composition formulation. The invention also provides a method for making tetrodotoxin stable in tetrodotoxin formulation, comprising the following steps: blending the tetrodotoxin, organic acid buffer solution and auxiliary material permitted to be used by pharmacopoeia according to a specific proportion so as to prepare a tetrodotoxin formulation used for injection. The tetrodotoxin formulation prepared by the composition preparation method of can be storedfor a long time under the condition of room temperature, thereby the problem that the tetrodotoxin formulation is unstable under the condition of the room temperature is solved.
WO2010062265A1 Therapeutic macrolide compounds and their use The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain macrolide compounds (for convenience, collectively referred to herein as "MC compounds"), which, inter alia, are useful in treatment of cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to treat proliferative conditions such as cancer, and in the treatment of diseases and conditions that are mediated by the regulation (e.g. inhibition) of cell proliferation, optionally in combination with another agent.
EP2754440A1 Medicinal agent for treating amyotrophic lateral sclerosis or preventing progression of phase of amyotrophic lateral sclerosis It is an object of the present invention to provide a novel pharmaceutical agent or method for treating ALS or suppressing the disease progress thereof, or treating symptoms caused by ALS or suppressing the disease progress thereof, wherein the agent can be administered particularly to patients obtaining high therapeutic effects, among ALS patients who require treatments. According to the present invention, there is provided a pharmaceutical agent for treating amyotrophic lateral sclerosis or suppressing the disease progress thereof or treating symptoms caused by amyotrophic lateral sclerosis or suppressing the disease progress thereof, which comprises, as an active ingredient, 3-methyl-1-phenyl-2-pyrazolin-5-one or a physiologically acceptable salt thereof, wherein the agent is administered by repeating a 14-day administration period and a 14-day drug holiday period, or by establishing an initial 14-day administration period and an initial 14-day drug holiday period and then repeating an administration period for 10 out of 14 days and a 14-day drug holiday period, and wherein a patient administered with the agent complies with specific criteria.
WO2007054216A1 Diaryl urea for treating pulmonary hypertension The present invention relates to pharmaceutical compositions for treating, preventing or managing pulmonary hypertension comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additionnal therapeutic agent.
CN1872070A Powder and injection preparation of left ofloxacin hydrochloric acid, and preparation method A powder injection of lavo-ofloxacin hydrochloride with high antibacterial effect is prepared from lavo-ofloxacin hydrochloride and excipient in weight ratio of 2:1. Its preparing process is also disclosed.
WO2014071824A1 4-quinazolinamine heterocyclic compound and use thereof A compound of (I), preparation methods therefor, and the use of the compound for preparing antineoplastic agents.
CN101697961A New cefmenoxime hydrochloride preparation for drug administration by injection and preparation method thereof The invention provides a new cefmenoxime hydrochloride preparation which is prepared by mixing cefmenoxime hydrochloride asepsis powder with cosolvent sodium bicarbonate asepsis powder, wherein the weight ratio of cefmenoxime hydrochloride (reduced to be pure cefmenoxime hydrochloride) to sodium bicarbonate is 1:0.1-1:0.3, preferably is 1:0.2 i.e. 0.1-0.3g of sodium bicarbonate asepsis powder is added into 1g of cefmenoxime hydrochloride (reduced to be pure cefmenoxime hydrochloride). After evenly mixed, asepsis split charging technology is adopted, and mixture is added into an aseptic soda-lime glass moulding injection bottle according to the labelled amount, the plug is pressed, a cover is rolled, full inspection is carried out, and the qualified product is packaged to obtain the cefmenoxime hydrochloride for injection. The product can overcome the problems of poor cefmenoxime hydrochloride dissolubility, poor stability, high impurity of relevant substance, polymer and the like, low content and the like of the existing cefmenoxime hydrochloride for injection and can better ensure clinic drug using safety. The invention belongs to the technical field of drug.
US20050004133 Inhibiting ligand gated ion channel vanilloid receptor (VR1); pain relievers; such as 6-(3,4-dichloro-phenyl)-N-(2-oxo-2,3-dihydro-1H-benzoimidazol-5-yl)-nicotinamide The present invention relates to compounds useful as modulators of the vanilloid receptor, and also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
CN102091275A Preparation method of vaginal antibacterial flushing fluid The invention relates to a preparation method of a vaginal antibacterial flushing fluid, which comprises the following steps: firstly, preparing raw materials: then, preparing stabilized chlorine dioxide; and finally, preparing a vaginal antibacterial flushing fluid product. The vaginal antibacterial flushing fluid produced by the invention can be directly used for foci to quickly sterilize pathogenic bacteria causing vaginitis, abnormal leukorrhea, vulvar inflammation, pruritus and peculiar smell, and especially can be used for thoroughly flushing and eliminating purulent secretions and rubbish-like lumps which are difficult to flush in deep vaginal front and back vaults. The product is safe, nontoxic, colorless and tasteless, does not have stimulation to the skin and vaginal mucosa, does not have side effects, can not pollute the skin, can not generate the drug resistance, can be preferably used for flushing twice per day for seriously infected persons, is convenient to carry, has the advantage of high treatment speed, is safe and sanitary, and is a female cleaning article for preventing infection.
CA2238430C Pyrazole derivatives, method for preparing same, and pharmaceutical compositions containing said derivatives Compounds of formula (I), wherein R1 is fluorine, hydroxy, (C1-5) alkoxy, (C1-5) alkylthio, hydroxy(C1-5)alkoxy, a -NR10R11 group, cyano, (C1-5) alkylsulphonyl or (C1-5) alkylsulphinyl; R2 and R3 are each (C1-4) alkyl or, taken together with the nitrogen atom to which they are attached, form a saturated or unsaturated 5- to 10-membered heterocyclic radical optionally substituted one or more times by (C1-3) alkyl or (C1-3) alkoxy; each of R4, R5, R6, R7, R8 and R9 is independently hydrogen, halogen or trifluoromethyl, and when R1 is fluorine, R4, R5, R6, R7, and/or R9 may also be fluoromethyl; with the proviso that at least one of substituents R4 or R7 is other than hydrogen; each of R10 and R11 is independently hydrogen or (C1-5) alkyl, or R10 and R11, taken together with the nitrogen atom to which they are attached, form a heterocyclic radical selected from pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl optionally substituted by (C1-4) alkyl; a method for preparing same, and pharmaceutical compositions containing said compounds, are disclosed. Said compounds have very high affinity for central cannabinoid receptors. (see formula I)
CN1810794A Prepn process and medicine composition of dewatered andrographolide The present invention relates to the preparation process and medicine composite of dewatered andrographolide with the expression as shown and possessing antipyretic and antiviral activity.
CN1843366A Burn-treating liquid The invention discloses a liquid for treating burns, which is prepared from the following raw materials (by volumetric ratio): medical liquid petrolatum 80-120, gentamycin sulfate 5-7.
WO2010129145A2 Methods and compositions for treating dry eye This invention relates to treatment of dry eye. In particular, the invention relates to methods and formulations for treating dry eye based on topical application of opioid antagonists such as naltrexone.
US20090318498 Piperidyl acrylamide antagonists of ccr2 The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5 and X are as defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is uveitis, including acute, recurring or chronic uveitis. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
US7422735 Use of crosslinked cationic polymers in skin cosmetic and dermatological preparations The invention relates to the use of at least one copolymer obtainable by (i) free-radically initiated copolymerization of a monomer mixture comprising (a) 1 to 99.99% by weight of at least one monomer chosen from N-vinylimidazoles and diallylamines optionally in partially or completely quaternized form; (b) 0 to 98.99% by weight of at least one neutral or basic water-soluble monomer which is different form (a); (c) 0 to 50% by weight of at least one unsaturated acid or unsaturated anhydride, (d) 0 to 50% by weight of at least one free-radically copolymerizable monomer which is different from (a), (b) or (c); and (e) 0.01 to 10% by weight of at least one monomer which acts as crosslinker and has at least two ethylenically unsaturated, nonconjugated double bonds; and (ii) subsequent partial or complete quaternization or protonation of the polymer in the case where the monomer (a) is unquaternized or only partially quaternized, as additive for skin cosmetic and dermatological preparations.
EP1702597A2 Drug delivery of phase changing formulation A formulation for delivering local anaesthetic topically is in an initial less than solid state and comprises water and tetracaine base, wherein as the water evaporates, the formulation converts to a coherent, peelable solid state.
CN103610666A Pramipexole dihydrochloride transdermal patch and preparation method thereof The invention particularly relates to a pramipexole dihydrochloride transdermal patch and a preparation method thereof, and belongs to the field of medicament preparation. A hydrophilic matrix mixed penetration enhancer is utilized, so that the condition that a medicament quickly releases within a long period of time at a constant speed, and achieves a relatively good permeation rate is guaranteed by adopting a multi-layer patch technology. The invention also discloses a preparation method of the pramipexole dihydrochloride transdermal patch, and the transparent patch which is good in uniformity is prepared.
WO2010029350A1 Treatment of fibrotic eye disorders Inhibitors of myosin activity are used to treat or prevent a fibrotic disorder of the eye, for example posterior capsule opacification (PCO).
US20100125051 Parenteral Formulations Comprising Sugar-Based Esters and Ethers The present invention relates to formulations for the parenteral administration of therapeutic agents, which contain sugar-based esters and ethers of fatty acids and fatty alcohols as surfactants. The formulations are advantageous for therapeutic agents which are insoluble or poorly soluble in water, and for reducing toxicity associated with common surfactants used in pharmaceutical formulations.
WO2006092417A1 6 -heteroaryl-1, 2, 3,4,4a, 1ob-hexahydro-phenanthridines as pde-4 inhibitors for the treatment of inflammatory disorders Compounds of a certain formula (I), in which R1 , R2, R3, R31, R4, R5, R51 and Har have the meanings indicated in the description, are novel effective PDE4 inhibitors.
US20130046013 Salicylate fatty acid derivatives Fatty acid conjugates of salicylate derivatives and compositions thereof are disclosed. Further disclosed are methods for treating various diseases comprising the administration of an effective amount of at least one compound according to the present disclosure.
US20080118563 Preparation of Chitin and Derivatives Thereof For Cosmetic and Therapeutic Use The invention relates to novel chitin derivatives and their use in medical treatments of plastic surgery, dermocosmesis and therapy, in particular it relates to natural chitin derivatives, like chitin in nanofibrillar form, oxychitin and other chemical derivatives of chitin, chitosan-hyaluronate and associations for use as subcutaneous fillers or skin protectants.
US7566727 2-(1-aza-bicyclo[2.2.2]oct-3-yl)-2,3-dihydro-isoindole-1-one/5,6-dihydro-furo[2,3-c] pyrrol-4-one derivative ligands for alpha 7 nicotinic acetylcholine receptor This invention encompasses nicotinic acetylcholine receptor reactive compounds in accord with formula (I) Wherein: D represents O; E represents CH2, NH, O or S; n is 1 or 2 and stereoisomers, enantiomers, in vivo-hydrolysable precursors and pharmaceutically-acceptable salts of such compounds, pharmaceutical compositions and formulations containing them, methods of using them to treat diseases and conditions either alone or in combination with other therapeutically-active compounds or substances, processes and intermediates used to prepare them, uses of them as medicaments, uses of them in the manufacture of medicaments and uses of them for diagnostic and analytic purposes.
CN1732920A Application of ligustilide in preparation of medicine for preventing and treating dysmenorrhea The invention discloses the use of ligustilide with a general formula (I) in preparing medicament for preventing and treating dysmenorrheal, wherein the ligustilide has evident analgesic action to acute and chronic pains.
CN101703504B Medicinal composition for vagina The invention relates to a medicinal composition for vagina. The composition comprises butoconazole nitrate, poloxamer, hydroxypropyl methylcellulose, Carbomer and other additives. The composition has the characteristics of good vagina mucosa adhesion and long-acting slow release, and in vivo and in vitro experiment results prove that the composition can continuously release the medicament for more than 72 hours.
WO2011110546A2 Pharmaceutical composition comprising an inhibitor of shp-2 and screening method The present invention relates to a pharmaceutical composition comprising at least one inhibitor of SHP-2, optionally together with pharmaceutically acceptable carriers, adjuvants, diluents and/or additives. The present invention also relates to screening methods for identification of a compound suitable as inhibitor of SHP-2.
CN103505444A Application of germacrone in preparation of liver cancer treatment medicines The invention provides an application of germacrone as a liver cancer treatment medicine. Results of experiments about the cytotoxicity of germacrone to HepG2 cells show that IC50 is about 160mum; and results of experiments about the detection of the influences of germacrone to liver cancer HepG2 cell cycle and apoptosis by using a flow cytometer show that germacrone can induce HepG2 cell G2/M cycle arrest and promote the cell apoptosis. Results of the detection of the cycle arrest and the apoptosis related protein expression situation by processing HepG2 cells through different concentrations of germacrone show that germacrone induces the HepG2 cell G2/M cycle arrest by reducing the cyclinB1 and CDK1 proteins and promotes the HepG2 cell apoptosis through p53 regulated mitochondrial apoptosis. Results of the detection of the ROS output of the germacrone processed HepG2 cells show that germacrone can promote the rise of the ROS output and cause the oxidative damages of the cells.
US6955821 Sustained release formulations of guaifenesin and additional drug ingredients The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin and at least one additional drug ingredient. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions has at least one additional drug ingredient. The modified release product has a maximum guaifenesin serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
EP1881982A1 Imidazolone phenylalanine derivatives as vla-4 antagonists Disclosed are compounds of the f ormula : and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21-R24 and Q are defined herein. These compounds bind VLA-4. Certain of these compound also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
US20060058351 Novel ligands that modulate LXR-type receptors and cosmetic/pharmaceutical applications thereof Novel compounds that are ligands of the LXR receptors have the following structural formula (I): and are formulated into pharmaceutical compositions useful in human or veterinary medicine, or alternatively into cosmetic compositions.
CN102988336A Use of TPCK (N-tosyl-L-phenylanyl chloromethyl ketone) in preparation of anti-lenticular opacity products The invention relates to a new application of N-tosyl-L-phenylanyl chloromethyl ketone (TPCK) and a composition thereof in the treatment of lenticular opacity. The efficacy of the TPCK in the aspects of preventing and treating the lenticular opacity and the like is mainly as follows: the anti-lenticular opacity action is realized by closing a channel which is positioned between nonessential mercapto of crystallin and profilin and can form a disulfide bond for causing nonspecific accumulation and further contain the formation of the macromolecular crystallin, a new medicament source and an application formulation are provided for chemical control of cataract, and the important reference value is further realized for preventing and treating other age-related eye diseases. The TPCK disclosed by the invention has the advantages of safety, low price, significant efficacy and stable nature, is suitable for large-scale production and commercial application in medicines, reagents and other industries and easy to popularize and apply, and further has good application prospects and significant social benefits and economic benefits.
CN103405455A Application of Chukrasone A in medicaments for treating laryngocarcinoma The invention discloses an application of Chukrasone A in preparing medicaments for treating laryngocarcinoma, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluation finds that the Chukrasone A also has a significant inhibitory effect on the growth of human laryngocarcinoma cell strains HEP-2, TU686, M2e and M4e. Therefore, the Chukrasone A can be used for preparing anti-laryngocarcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating laryngocarcinoma provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to laryngocarcinoma cells.
CN101543525B Beauty composition containing vaccinium vitis-idaea extract and application thereof The invention relates to a beauty composition containing a vaccinium vitis-idaea extract and application thereof to skin beauty. The invention provides the vaccinium vitis-idaea extract, which contains components of anthocyanin, procyanidin, resveratrol and polyphenols such as catechin and the like. The invention also relates to the application of the vaccinium vitis-idaea extract to the beauty, including but not limited whitening, color fleck removing, wrinkle removing, skin smoothness strengthening, and skin sensitivity improving. The invention also discloses a medicament, the beauty composition and food which are prepared from the vaccinium vitis-idaea extract. Compared with the prior cosmetics, the vaccinium vitis-idaea extract has better effect and higher safety.
US20120232066 Compositions for reducing risk of adverse events caused by drug-drug interactions The present disclosure provides a composition comprising a GABAA agonist and a GI enzyme inhibitor. The present disclosure also provides a composition comprising (a) a GI enzyme inhibitor and (b) a first drug that interacts with a second drug to produce an adverse effect when the second drug is co-ingested as a GI enzyme-cleavable prodrug with the first drug. Such an interaction can be additive or synergistic.
CN103417565A Application of depolymerized holothurian glycosaminolycan in preparing drugs for curing and preventing thrombotic diseases The invention discloses an application of depolymerized holothurian glycosaminolycan in preparing drugs for curing and preventing thrombotic diseases. The weight average molecular weight of depolymerized holothurian glycosaminolycan is at least one kind of 55000 Da to 96000 Da. It has been testified by a large amount of experiments that the depolymerized holothurian glycosaminolycan is capable of being safely and effectively applied to the prevention and cure of thrombotic diseases.
CN102579366A Method for preparing Etofibrate sustained-release pellet The invention provides a method for preparing an Etofibrate sustained-release pellet, which comprises a pill-contained core, a solubilizing layer and a sustained-release layer. The solubilizing layer which consists of Etofibrate and solubilizing materials coats the Etofibrate pill-contained core, then the solubilizing materials are adopted to coat the pellet of the Etofibrate solubilizing layer, and the Etofibrate sustained-release pellet which sustainably releases for 24h is prepared.
US20110081337 Function of gpr4 in vascular inflammatory response to acidosis and related methods The present invention relates to methods for the treatment of inflammation. Specifically, disclosed herein are methods to inhibit vascular inflammatory responses by inhibiting the proton-sensing GPR4 receptor. Such methods can be utilized, most preferably, in pharmaceutical compositions to modulate inflammation in acidosis-related diseases.
CA2615427A1 Oral contraception with trimegestone The invention relates to a method for contraception comprising the administration of trimegestone in combination with ethinyloestradiol to a woman of child-bearing age on at least 21 successive days, beginning on day 1 of the menstrual cycle, wherein on at least one of the at least 21 successive days the daily dose of trimegestone is more than 500 ~g.
CA2837429A1 Pharmaceutical composition comprising a trpa1 antagonist and a beta-2 agonist The present patent application relates to a pharmaceutical composition comprising a transient receptor potential ankyrin-1 receptor ("TRPA1") antagonist and a beta-2 adrenergic receptor agonist ("beta-2 agonist").
CN102861057A Application of Houttuynoid D in skin cancer treatment medicine The invention relates to application of Houttuynoid D in preparing skin cancer treatment medicine, which belongs to the technical field of new application of the medicine. According to the assessment on the antineoplastic activity through in-vitro MTT method, Houttuynoid D has an obvious inhibiting effect on the growth of human skin cancer cell strains A431, HME1, A375 and SK23. Therefore, Houttuynoid D can be used for preparing the skin cancer treatment medicine, and has a favorable development and application prospect. The application of Houttuynoid D in preparing the skin cancer treatment medicine, which is provided by the invention, is disclosed for the first time, and because the skeleton type belongs to brand-new skeleton type, the inhibiting activity of Houttuynoid D to skin cancercells is extremely strong.
US7112686 Precipitation from mother liquors by adding bases or acid addition salts to solution of citalopram The invention relates to a process for the preparation of racemic citalopram free base or an acid addition salt thereof and/or R- or S-citalopram as the free base or an acid addition salt thereof by separation of a mixture of R- and S-citalopram with more than 50% of one of the enantiomers into a fraction consisting of racemic citalopram and/or a fraction of S-citalopram or R-citalopram characterized in that i) citalopram is precipitated from a solvent as the free base or as an acid addition salt thereof; ii) the precipitate formed is separated from the mother liquor; iia) if the precipitate is crystalline it is optionally recrystallised one or more times to form racemic citalopram, and then optionally converted into an acid addition salt thereof; iib) if the precipitate is not crystalline, steps i) and ii) are optionally repeated until a crystalline precipitate is obtained and the crystalline precipitate is recrystallised one or more times to form racemic citalopram, and then optionally converted into an acid addition salt thereof; iii) the mother liquor is optionally subjected to further purification and S-citalopram or R-citalopram is isolated from the mother liquor and optionally converted into an addition salt thereof.
CA2172162C Optically active imidazolidinone derivative and process for producing the same The invention relates to a stereoisomer 3-(R)-imidazolidinonyl piperidine of the following structure: wherein R and R1, independently, denote hydrogen atoms, halogen atoms, lower alkyl groups which may be substituted by halogen atoms, lower alkoxy groups, lower alkylthio groups; lower alkoxycarbonyl groups, vitro groups, amino groups or cyano groups, and n denotes 1 to 4, or an acid addition salt thereof.These optically active imidazolidinone derivatives have cholinergic activity (a muscarine M1 activity) and are useful for treating senile dementia. The invention also relates to pharmacologically acceptable acid-addition salts of these derivatives, and processes for producing them.
US20100055176 Method of Treating Fibromyalgia or Associated Functional Symptoms of Fibromyalgia The invention relates to a method of treating fibromyalgia or associated functional symptoms of fibromyalgia using a 1-acylpiperidine substance P antagonist, the 1-acylpiperidine substance P antagonist comprising a compound of formula wherein X and Y are each independent of the other N and/or CH, and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl and for each compound, pharmaceutically-acceptable salts thereof.
US20100196479 METHODS AND COMPOSITIONS COMPRISING AT LEAST ONE ALPHA3 BETA4 nAChR ANTAGONIST OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF The present invention is directed to methods and formulations for treating, modifying, and/or managing gastrointestinal secretion, and intestinal conditions that cause the same. Methods of using at least one α3 β4 nAChR antagonist and formulations comprising at least one α3 β4 nAChR antagonist, or pharmaceutically acceptable salt thereof, are included.
CN103006703A Sodium phosphate medicament The invention discloses a sodium phosphate medicament. The medicament comprises sodium dihydrogen phosphate monohydrate, disodium hydrogen phosphate heptahydrate, glycerol, sodium saccharin, sodium benzoate, ginger essence, lemon essence and purified water in a weight ratio of 480g:180g:15g:3.3g:0.35g:0.5ml:1000ml. The medicament has the advantage that a better medical treatment effect is achieved.
CN1857294A Antipyretic analgesic The present invention provides a kind of antipyretic analgesic and relates to medicine preparing technology. The antipyretic analgesic is prepared with acetaminopher, astragaloside, caffeine, chlorphenamine maleate, and cloperastine hydrochloride, and through gradual dilution and mixing. The antipyretic analgesic of the present invention has high antipyretic and analgesic effect, high cold treating effect and less toxic side effect.
CN101361708A Morphine sulphate suppository and preparation method thereof The invention discloses a morphine sulfate suppository and a preparation method thereof. The suppository is prepared by morphine sulfate, hard fat, TW-80, microcrystalline cellulose, siliciiDoxydum, butylhydroxyanisolBHA and 2, 6-d-tert-butyl-p-cresol(BHT) according to certain weight percent, and the preparation method comprises the steps of: A. sifting out the main drug of morphine sulfate and the accessories of siliciiDoxydum, microcrystalline cellulose, butylhydroxyanisolBHA and 2, 6-d-tert-butyl-p-cresol(BHT) for spare use; B. heating, melting and mixing evenly the substrate of the hard fat and the hard fat; C. adding the sifted accessories and TW-80 under even stirring into the melted substrate and morphine sulfate and evenly stirring the mixture with heat preservation; and D. carrying out stirring and moulding on the mixture with temperature reduction, and cooling. The morphine sulfate suppository has the advantages of reasonable formulation, prominent healing effect, simple and convenient use and safe and effective clinical application and is applicable to moderately severe advanced cancer patients, and the postoperative pain of the patients can be stopped.
CN103432115A Application of Chukrasone B in preparation of medicaments for treating skin cancer The invention discloses application of Chukrasone B in preparation of medicaments for treating skin cancer and belongs to the technical field of novel application of medicaments. An in-vitro MTT (methyl thiazolyl tetrazolium) anticancer activity evaluation discovers that Chukrasone B has a remarkable inhibition effect on the growth of human skin cancer cell strains A431, HME1, A375 and SK23. Therefore, Chukrasone B can be used for preparing anti-skin cancer medicaments and has great development and application prospect. The application of Chukrasone B in preparation of medicaments for treating skin cancer is disclosed for the first time, and the frame type belongs to a brand-new frame type, so that the inhibition activity of the Chukrasone A to skin cancer cells is unexpectedly strong.
CN102958935A Macrocyclic integrase inhibitors The invention relates to a compound having formula (I) and pharmaceutically acceptable salts or solvates thereof, their pharmaceutical formulations and use as HIV inhibitors.
WO2005110392A1 Methods of modulating flt3 activity Disclosed are methods for modulating FLT3 activity, including methods for the treatment of conditions characterized by abnormal FLT3 expression, such as leukaemia.
US20100256171 Selective serine/threonine kinase inhibitors Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.
CN103462981A Application of spirooliganones B in preparation of medicine promoting small intestine peristalsis The invention relates to the application of spirooliganones B in preparation of the medicine promoting the small intestine peristalsis. The pharmacological experiment shows that the spirooliganones B has good effect on promoting the small intestine peristalsis. The application of spirooliganones B in preparation of the medicine promoting the small intestine peristalsis is disclosed for the first time. The spirooliganones B belongs to a brand new matrix type, has the advantages of being high in activity of promoting the small intestine peristalsis and prominent in substantive features, and makes remarkable progress in preparation of the medicine promoting the small intestine peristalsis.
EP2209790A2 Equilibrative nucleoside transporter ent1 inhibitors The present invention is related to novel compounds of formula (I) having equilibrative nucleoside transporter ENTl inhibiting properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the inhibition of ENTl receptors in animals, in particular humans.
CN1911234A Reversing agent for drug-fast during treating tumor with multiple medicines A pregnane compound for reversing the resistance of cancer cells to multiple medicines is a pregnane derivative, that is, the derivative of tenacigenin B or C and the derivative of dihydrosarcostin.
CN103211772A Etoposide lyophilized powder for injection The invention relates to an etoposide lyophilized powder for injection. The powder can overcome the defects of etoposide, improve the bioavailability of etoposide, is convenient to use, can be absorbed fast, and can come into play rapidly. By screening the prescription of the etoposide lyophilized powder for injection, the invention finds that the combined use of a specific excipient with an antioxidant and a chelating agent at the same time can generate a finished product of etoposide lyophilized powder for injection with the advantages of high stability, fewer impurities, little side effect, high safety, convenient storage and use, low production cost, and the like.
WO2007114239A1 ANTI-CANCER AGENT COMPRISING DGKα INHIBITOR [PROBLEMS] To provide a novel anti-cancer agent. [MEANS FOR SOLVING PROBLEMS] Disclosed are an anti-cancer agent, an apoptosis inducer in a cancer cell, an apoptosis inducer in a melanoma cell, and a suppressor of the expression of NF-ϰB, each of which comprises a DGKα inhibitor as an active ingredient. Examples of the DGKα inhibitor include an anti-DGKα antibody, and an antisense oligonucleotide, ribozyme or siRNA for a DGKα gene. Also disclosed is a method for identification of a candidate substance for an anti-cancer agent, an apoptosis inducer in a cancer cell, an apoptosis inducer in a melanoma cell, or a suppressor of the expression of NF-ϰB. The method comprises contacting a substance to be examined with a cell capable of expressing DGKα and determining whether or not the substance can inhibit the expression and/or function of DGKα.
US20130040979 Ccr1 inhibitors useful for the treament of multiple myeloma and other disorders The invention relates to the use of inhibitors of CCR1 for the treatment of cancers and osteolytic bone disorders. In some embodiments, the invention relates to methods for the treatment of multiple myeloma, smoldering multiple myeloma and secondary bone cancers.
CN1660096A Effervescence tablet of fibrauretine and preparation method An effervescent tablet of huangtensu is prepared from huangtensu or other alkaloid mixture containing heuangtensu, magnesium stearate, polyethylene glycol PEG, and talc powder or superfine silica gel powder through proportionally mixing and tabletting.
CN1839809A Novel uses of (E) -4,4íõ-dimethoxy styrene and its composition containing same The invention discloses an (E)-4,4'-dimethoxybenzene ethylene represented by formula (I) and its salts, the use in preparing oxidation resistant or antisenescent drugs, health foods and cosmetics, as well as the medicinal composition and health foods containing the compound.
CN101347414B Divisible galenical preparation form capable of controlling release of active ingredient The invention relates to a dividable galenical preparation form capable of controlling and releasing active ingredient, in which the undivided galenical preparation form has same dissolution with part of said preparation form obtained by redivision.
CA2588942A1 The original sheridan cecil spicer scalpe loosers and scalpe healing hair restoration solution and healthy haire management system It is known that in order for the scalp to be healed and for it to produce hair, that the scalp must be cleansed, the follicle of the hair must be unplugged and that the dermatitis of the sebaceous glands and related haire follicle, inflammation sores and surrounding skin and scalp be healed.
CA2752473A1 Composition and method for treating ulcers The composition for the treatment of ulcers includes ground charcoal, ground mustard seed and an edible salt dissolved or suspended in an edible oil. A single effective therapeutic dosage of the composition includes approximately 4,000 mg of the ground charcoal, approximately 2,500 mg of the ground mustard seed, approximately 550 mg of the edible salt, and approximately 15 ml of the edible oil. The effective therapeutic dosage is delivered to the patient orally, and may be provided to the patient as a tablet or capsule, or as a liquid mixture.
US20100047260 Methods and Compositions Relating To a Vaccine Against Prostate Cancer An object of the invention is to provide methods and compositions relating to a vaccine against prostate cancer which includes a non-human-primate PSA for administration to humans to provide an immune response against human PSA. More generally, an object of the invention is to provide methods and compositions relating to using a non-human primate xenogeneic antigen (e.g. protein) in a human, wherein, with respect to the non-human primate xenogeneic antigen that is used, there are relatively few interspecies differences between the non-human primate xenogeneic antigen and the human self antigen in order to induce an optimal immune response in the human to its native self antigen.
US20110288093 Compounds, Compositions, and Methods Comprising Pyridazine Sulfonamide Derivatives The present invention relates to methods for treating a disease in an animal, which disease is responsive to blocking of chloride channel by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-3 or encompassed by formula I-III) or compositions thereof
WO2006059210A3 Fused bicyclic pyrrols as hmg-coa reductase inhibitors HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidenuc compounds are provided. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided.
WO2006089881A1 Use of phenanthrene derivatives as anti-inflammatory agents, synthesis method and intermediate products The invention concerns the use of phenanthrene derivatives of formula (I), wherein R1 and R2 represent a hydroxyl or methoxy radical; R3 represents a hydrogen atom or a hydroxyl radical optionally protected by a suitable protecting group; R4 represents a hydrogen atom or a methoxy radical, for making a medicine for inhibiting inflammatory reactions. The invention also concerns a method for dermo-cosmetic skin treatment which consists in applying on the skin a composition comprising at least one phenanthrene derivative of formula (I). Finally, the invention concerns a method for synthesis of said phenanthrenes of formula (I) as well as the intermediate products.
WO2014099900A1 Composition and methods for treating or preventing lung diseases As described below, the present invention features compositions and methods for treating or preventing lung disease (e.g., chronic obstructive pulmonary disease (COPD), emphysema, and other conditions associated with cigarette smoke exposure) are urgently required.
CA2326198C Cosolvent formulations Stable pharmaceutical formulations of a therapeutic agent, a low molecular weight alcohol and a glycol derivative are disclosed. Preferred formulations include 19-nor-1.alpha.,3.beta.,25-trihydroxy-9,10-secoergosta-5,7(E),22(E)-triene.
EP1849462A2 A method of alleviating signs and symptons of Spasticity The present invention provides a method for alleviating signs and symptoms of spasticity in human patients comprising orally administering to said human patients once in a day a controlled drug delivery system comprising an effective daily dose of baclofen or its pharmaceutically acceptable salt wherein said method is associated with reduced level of sedation in said patients as compared to levels of sedation associated with conventional baclofen therapy with immediate release tablets administered three times a day on the same total daily dose.
CN103356700A Joint maintaining ointment The invention belongs to the preparation field of medical external application medicines and particularly relates to a joint maintaining ointment. The joint maintaining ointment comprises the following three raw materials in parts by weight: 15-25 parts of emu oil, 45-75 parts of MSM (dimethyl sulfone) and 25-35 parts of glucosamine sulfate; the components are directly mixed to obtain a paste product; and 8-12 parts of titanium dioxide are further added in the raw materials. The preparation process of the joint maintaining ointment is simple. The joint maintaining ointment is convenient to use, has good permeability and is capable of improving the blood circulation of joints, promoting the absorption of nutriments and relieving the paint of the joints.
US20100297083 Polynucleotides and Polypeptide of Human KV1.3, Compositions Comprising Same and Methods of Using Same An isolated polypeptide comprising, contiguously, a first amino acid sequence being at least 90% homologous to amino acid coordinates 1-398 of SEQ ID NO: 2, a tryptophan residue and a second amino acid sequence being at least 90% homologous to amino acid coordinates 400-523 of SEQ ID NO: 2. Also provided are polynucleotide sequences encoding this polypeptide and uses of same in the treatment of medical conditions associated with ion channel insufficiency.
WO2013159166A1 Pharmaceutical oral dosage form for preventing vascular diseases, tablet as pharmaceutical dosage form and gelatin capsule as pharmaceutical dosage form The present invention broadly relates to pharmaceutical oral dosage forms directed to therapeutic use for preventing cardiovascular and cerebrovascular diseases in mammals, preferably humans. More particularly, the invention relates to a tablet that comprises (a) one or more HMG-CoA reductase inhibitors, (b) one or more angiotensin II receptor antagonists and (c) one or more diuretics of the thiazide class.
EP1718630A1 DIBENZO CHROMENE DERIVATIVES AND THEIR USE AS ER&bgr; SELECTIVE LIGANDS This invention provides estrogen receptor modulators of fomula (I), having the structure where R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification.
CN102133182A Epoprostenol liposome and preparation method thereof The invention relates to epoprostenol liposome and a preparation method thereof. In the liposome, the weight ratio of the epoprostenol to a phospholipid material is 1:4 to 1:200. A membrane dispersion-high pressure homogenizing method is adopted for preparation, the prepared liposome not only solves the stability problem of a medicament, but also reduces the irritation of intravenous administration, thus improving the safety in clinical medication.
CN103054887A Patch for treating oral ulcer The invention discloses a patch for treating oral ulcer. Every 625 patches are prepared from the following raw materials: 0.5*10<6> to 2*10<6>IU of neomycin sulfate, 0.5 to 2g of clotrimazole, 0.1 to 1g of tetracaine hydrochloride, 1 to 8mg of betamethasone, 2 to 10g of borneol, 2 to 10g of mannitol, 2 to 10g of sodium carboxymethylcellulose, 10 to 20mL of ethanol, 0.05 to 2mL of glycerol and 10 to 20mL of purified water. The medicine is simple in component and low in cost, has an obvious curative effect on patients suffering from recurrent oral ulcer and does not have any toxic or side effects.
CN103570684A Phenylamine benzimidazole derivative and application of phenylamine benzimidazole derivative in preparation of anticoagulation medicine The invention relates to phenylamine benzimidazole derivative and application of the phenylamine benzimidazole derivative in preparation of an anticoagulation medicine. The phenylamine benzimidazole derivative is an ideal thrombin inhibitor and can be used for preventing or treating thrombogenesis and other indications, comprising auricular fibrillation, acute coronary syndrome, acute symptomatic venous thrombosis, cerebral arterial thrombosis and the like. The phenylamine benzimidazole derivative compound produces less first pass effect, is high in effective biological availability and has the advantages of low dosage and less side effect when being used for treating indications related to functions of thrombin.
US7323569 N-cyclopropylmethyl-N-7-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-2-ethylpyrazolo[1,5-a]pyridin-3-yl-N-tetrahydro-2H-4-pyranylmethylamine. A compound represented by the formula: [wherein R1 is methoxy, methylthio, ethyl, etc.; R5 and R6 are each independently cyclopropylmethyl, (4-tetrahydropyranyl)methyl, etc.; and two of R40, R41 and R42 are C1-6 alkoxy while the remaining one is methoxymethyl, etc.], a salt thereof, or a hydrate of the foregoing. This compound has excellent antagonism against corticotropin-releasing factor receptor.
WO2007124005A3 Methods for treating bone associated diseases by the use of methionine aminopeptidase-2 inhibitors The instant invention provides the use of METAP-2 inhibitors to manufacture pharmaceutical compositions for treating a subject suffering from bone associated diseases, such as osteoporosis.
US20070054882 Male anti-fertility agents Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.
WO2005026153A1 Quinazoline-2, 4-diones as antibacterial agents Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.
CN103565774A Glipizide controlled release composition as well as preparation method thereof The invention relates to a glipizide controlled release composition which consists of a double-layer tablet core and a semipermeable membrane controlled release coating membrane. The double-layer tablet core consists of a medicine containing layer and a boosting layer, wherein the medicine containing layer and the boosting layer of the composition are pelletized by a water suspension. The invention further relates to a preparation method of the glipizide controlled release composition. The preparation method comprises the following steps: pelletizing the medicine containing layer; pelletizing the boosting layer; preparing the double-layer tablet core; coating; and punching, wherein the medicine containing layer and the boosting layer are pelletized by the water suspension. The glipizide controlled release composition prepared by the preparation method provided by the invention is uniform in particle distribution, good in tabletting and forming effect, uniform in content, low in residual rate of organic solvents and good in dissolving out effect. The preparation method is simple and feasible and is favorable for industrial production.
CN1895236A Oral-cavity adhering sheets and production thereof An oral paster with high bactericiding effect is prepared through proportionally mixing metronidazole, auxiliary and flavouring, stirring, granulating, baking, pressing and packing.
WO2013052006A8 Parp-1 inhibitors We describe a nucleic acid comprising the sequence RNNWCAAA, in which R is independently G or A, N is independently T, C, G or A and W is independently T or A, suitable for the treatment or prevention of hepatitis B or cancer. N at position 3 may be C, A or T, preferably A or T, more preferably T; N at position 2 may be C; W at position 4 may be T; and R at position 1 may be A. The nucleic acid may have the sequence ACATCAAA or ACTTCAAA.
WO2005105852A1 Novel arabinogalactan, substance with antidiabetic activity and method of use thereof A highly effective safely ingestible antidiabetic medicine or functional food with antidiabetic activity, provided as a result of finding a novel ingredient with antidiabetic activity contained in food. In particular, there is provided an arabinogalactan extracted from the skin of white sweet potato with a water base solvent and purified, comprising a skeleton of β1,6-bonded Gal sugar chain highly branched by β1,3-bonds so that (1) αAraf is α1,3-bonded or (2) αAraf(1→5)αAraf is α1,3-bonded, as side chains, to about 65 to 75% of Gal’s constituting the skeleton and that (3) αRha(1→4)βGlcUA is β1,6-bonded to some or all of terminal Gal’s of the skeleton, and having a molecular weight of 10×104 to 20×104, wherein the constitutional ratio of rhamnose to glucuronic acid is approximately 1:1, the constitutional ratio of arabinose to galactose approximately 1:2 and the constitutional ratio of rhamnose to arabinose approximately 1 : 5 to 6. This arabinogalactan is used as a medicine with antidiabetic activity.
US20120095051 Curcumin analogues as zinc chelators and their uses This invention provides a compound having the structure wherein α, β, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NFκ-B activation in a population of cells.
CN103301063A S (+) -flurbiprofen axetil emulsion for injection The invention discloses application of a low-dosage esflurbiprofen axetil emulsion for injection. For the S (+) -flurbiprofen axetil emulsion for injection provided by the invention, when a certain curative effect is realized, the needed dosage of the S (+) -flurbiprofen axetil emulsion for injection is only 25%-75% of the dosage of the market flurbiprofen axetil emulsion, correspondingly, the clinic treatment dosage of the S (+) -flurbiprofen axetil emulsion for injection is 25%-75% of the market flurbiprofen axetil emulsion.
US8048646 NELL peptide expression systems and bone formation activity of NELL peptide The invention generally relates to a bone growth factor, and more particularly to compositions including NELL1, articles of manufacture including NELL1 and methods of using NELL1 to induce bone formation. This invention also provides methods for the expression and purification of NELL1 and NELL2 peptides.
CN1768873B Apparatus and method for electroporation mediated delivery for drugs and genes This invention is a method, and apparatus (100) for in vivo electroporation therapy. Using electroporation therapy (EPT) as described in the invention, tumors treated by a combination of electroporation using the apparatus (100) of the invention, and a chemotherapeutic agent caused regression of tumors in vivo. In one embodiment, the invention provides a method of EPT utilizing low voltage, and long pulse length for inducing cell death. One embodiment of the invention includes a system for clinical electroporation that includes a needle array electrode (114) having a 'keying' element that determines the set point of the therapy voltage pulse, and/or selective array switching patterns. A number of electrode applicator designs permit access to, and treatment of a variety of tissue sites. Another embodiment provides a laparascopic needle applicator that is preferably combined with an endoscope for minimally invasive EPT.
CN101897731A External spraying agent based on complex biological acid The invention relates to an external spraying agent based on complex biological acid, which is designed for solving the technical problem that the existing common external skin spraying agents have functions of anti-inflammation and sterilization and promoting blood circulation and removing blood stasis, but do not have a regeneration function on skin cells. The external spraying agent is prepared by a method comprising the following steps: taking the following components by weight percent: 90-95% of purified water filtered by an R-module, 1-8% of medical glucose, 0.5-2.0% of agar and 0.5-2.5% of lactic acid bacteria; enlarging and reproducing the lactic acid bacteria to a complex bacterium through fermentation of biological bacteria-lactic acid bacteria; and finely filtering the supernatant of the formed complex bacterium to obtain the external spraying agent. A detection result from safety and agricultural product environmental quality detection center in Shenyang institute of ecology of Chinese Academy of Sciences indicates that the spraying agent contains eighteen amino acid small peptides, has extremely ideal efficacy on treating mosquito bite, whelk, various dermitis, dermatophytosis, eczema, acne and the like except anti-inflammation and sterilization and promoting blood circulation and removing blood stasis functions, especially has activation and restoration functions on the skin cells for burn, scald, skin fester, intractable psoriasis and the like, and if probiotic oral liquid is orally administrated with the spraying agent, the clinical effect is better and the cure rate is higher.
WO2012059572A1 COMBINATION OF ATOMIC QUANTUM CLUSTERS (AQCs) AND ANTINEOPLASIC DRUGS, AND ITS USE IN THE PREVENTION AND/OR TREATMENT OF CELL PROLIFERATIVE DISORDERS The present invention relates to a combination of at least one atomic quantum cluster (AQC) or a hydrate thereof, and at least one antineoplasic drug, and to the use of such combination as a pharmaceutical combination in the prevention and/or treatment of cell proliferative disorders.
CN101337920A Phenylalanyl pyrrolidine derivates, preparation method and application thereof The invention discloses a 2-pyrrolidine substitution-hydrocinnamoyl pyrrolidine derivant which is the compound in formula 1 or an acceptable salt thereof in pharmacy, wherein, R1 or R2 is respectively hydrogen, cyano-group, acidic group, ester group, acyl group, amide group or substitution amide group independently; the hexagram symbol stands for a chiral centre. The invention further discloses a method for preparing the compound and the application thereof for preparing or preventing noninsulin-dependent diabetes mellitus, adiposis, arthritis or other glucose tolerance abnormality diseases.
US20050282769 Inhibitors of adenosine kinase for the treatment of optic nerve and retinal damage Methods for preventing and treating damage to the optic nerve and/or retina with adenosine kinase inhibitors are disclosed.
WO2011153939A1 Agomelatine intermediates and preparation method thereof Intermediate compounds for preparation of agomelatine and preparation methods thereof are provided. Also provided are two novel intermediate compounds. The method is simple to manipulate, well-controlled, suitable for industrial production and has a high purity without complicated operations such as rectification and column chromatography separation. Meanwhile, preparation methods of the two new intermediates themselves are simple and have a high yield.
US20120122977 Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, X, X1, s and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
US8119631 Inhibitors of interleukin-1β converting enzyme The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.
CN102225903A Amidino guanido substituted aromatic heterocyclic copmound and synthesis and use thereof The invention relates to an amidino guanido substituted aromatic heterocyclic compound represented by the general formula (I), wherein, R1, R2 can represent same or different groups, and can substitute the group at any position of the hetero-aromatic ring, can be represented as: -O-R3, -S-R3, -COOR3, -COR3, -O-COR3 and -NH-COR3, m represents a natural number such as 0,1or 2; R3 represents a hydrogen atom, linear alkyl or branched alkyl, substituted or non-substituted aromatic group or aromatic heterocyclic ring; R4 and R5 represent a hydrogen atom, linear alkyl or branched alkyl, aromatic group or aromatic heterocyclic ring; A ring represent a cycloaliphatic ring, aromatic ring, aromatic heterocyclic ring or fused heterocycle; X and Y represent carbon, nitrogen, oxygen, sulfur and the like and can be any position on the ring; B represents -COO-, -CONH-, -COS-, -CSO-, -CSNH-, -CSS-, -OCO-, -NHCO-, -SCO-, -OCS-, -NHCS-, -SCS- or the like, and n represents a natural number such as 0,1or 2. The compound disclosed in the invention has stable property, can inhibit tryptic activity proved by enzymatic activity experiments, and can be used for preparing medicines for treating acute or chronic pancreatitis.
US20100016357 Use of Beta-Aminoalcohols for the Treatment of Inflammatory Disorders and Pain Compounds that may be used for the treatment or prevention of a condition associated with T-cell proliferation or that is mediated by pro-inflammatory cytokines are of formula (I): wherein at least one of R1, R2 or R3 is not H and each is independently H, alkyl, CF3, CONH2, CN, halogen, NH2, NO2, NHCHO, NHCONH2, NHSO2alkyl, SOMe, SO2NH2, Salkyl, or CH2S02alkyl; and R4 is H or alkyl; or a salt thereof.
WO2006092430A1 Selective inhibitors of human corticosteroid synthases The invention relates to compounds for selectively inhibiting human corticosteroid synthases CYP1 1 B1 and CYP1 1 B2, and to the production and use thereof for treating hypercortisolism, diabetes mellitus, hyperaldosteronism, cardiac insufficiency, myocardial fibrosis, depression, age-related cognitive decline and metabolic syndrome.
US20060122124 Therapeutic agent Agent for the depletion of an unwanted protein population from the plasma of a subject, which agent comprises a plurality of ligands covalently co-linked so as to form a complex with a plurality of the proteins in the presence thereof, wherein at least two of the ligands are the same or different and are capable of being bound by ligand binding sites present on the proteins, wherein the agent is a non-proteinaceous agent other than a D-proline of the formula wherein R is the group R1 is hydrogen or halogen; X is —(CH2)n—; —CH(R2)(CH2)n—; —CH2O(CH2)n—; —CH2NH—; benzyl, —C(R2)═CH—; —CH2CH(OH)—; or thiazol-2,5-diyl; Y is —S—S—; —(CH2)n—; —O—; —NH—; —N(R2); —CH═CH—; —NHC(O)NH—; —N(R2)C(O)N(R2)—; —N[CH2C6H3(OCH3)2]—; —N(CH2C6H5)—; —N(CH2C6H5)C(O)N(CH2C6H5)—; —N(alkoxyalkyl)-; N(cycloalkyl-methyl)-; 2,6-pyridyl; 2,5-furanyl; 2,5-thienyl; 1,2-cyclohexyl; 1,3-cyclohexyl; 1,4-cyclohexyl; 1,2-naphthyl; 1,4-naphthyl; 1,5-naphthyl; 1,6-naphthyl; biphenylen; or 1,2-phenylen, 1,3-phenylen and 1,4-phenylen, wherein the phenylen groups are optionally substituted by 1-4 substituents, selected from halogen, lower alkyl, lower alkoxy, hydroxy, carboxy, —COO-lower alkyl, nitrilo, 5-tetrazol, (2-carboxylic acid pyrrolidin-1-yl)-2-oxo-ethoxy, N-hydroxycarbamimidoyl, 5-oxo[1,2,4]oxadiazolyl, 2-oxo-[1,2,3,5]oxathiadiazolyl, 5-thioxo[1,2,4]oxadiazolyl and 5-tert-butylsulfanyl-[1,2,4]oxadiazolyl; X′ is —(CH2)n—; —(CH2)nCH(R2)—; —(CH2)nOCH2—; —NHCH2—; benzyl, —CH═C(R2)—; —CH(OH)CH2; or thiazol-2,5-diyl; R2 is lower alkyl, lower alkoxy or benzyl and n is 0-3, or a pharmaceutically acceptable salt or mono- or diester thereof.
WO2011092671A1 Proline derivatives for use in the treatment of diabetes The present invention provides novel heterocyclic compounds and methods of preparing such compounds. The compounds of the invention are useful for palliative, curative or prophylactic treatment of diseases or conditions of diabetes and/or hypertension. This invention also relates to pharmaceutical compositions containing the compounds of the present invention, and methods for palliative, curative or prophylactic treatment of diseases or conditions of diabetes and/or hypertension. The present invention also provides pharmaceutical compositions consisting of the heterocyclic compounds along with one or more dyslipidemic agents, antiobesity agents, anti-hyperglycemic agents, antihypertensive agents and anti-inflammatory agents.
CN103040843A Solid dispersion containing clobetasol propionate and tretinoin and preparation method thereof The invention provides a solid dispersion of compound clobetasol propionate and tretinoin. The solid dispersion of clobetasol propionate and tretinoin is prepared by utilizing lipid material, wherein the medicament is dispersed in the solid dispersion in a molecule manner, is heated to be fused when used, to form uniform medicament solution, and the medicament is uniformly distributed in each part in the solution. A proper amount of pharmaceutically acceptable accessory is added to prepare an ointment. The solid dispersion can be uniformly dispersed in the ointment, and the ointment would not appears layered phenomenon and always maintains uniform medicament content in the whole system even in the case of 60 DEG C. Shown in a skin retention test, the skin retention amount of the solid dispersion ointment is obviously higher than that of a common ointment, which is in favor of raising pharmaceutical effect and reducing toxic and side effect.
US20110082132 [4-(1-amino-ehtyl) - cyclohexyl] -methyl-amine and [6-(1-amino-ehtyl) -tetrahydro-pyran-3-yl] -methyl-amine derivatives as antibacterials The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy or halogen; U, V and W each represent CH, or one of U, V and W represents N and the others each represent CH; A represents CH2 or O; G is CH═CH—E wherein E represents a phenyl group mono- or di-substituted with halogen, or G is a group of one of the formulae hereafter wherein Z represent CH or N, Q represents O or S and K represents O or S; and salts of such compounds.
US7125911 Autonomic nerve regulating agent The autonomic nerve regulating agent of the present invention, which, has sedative action, sleep inducing action, and stress mitigating action in individuals, regardless of individual variation in sensitivity to or preference for fragrance, contains as an active ingredient a sesquiterpene alcohol with a boiling point of 250° C. or higher, particularly cedrol.
CA2159419C Solid pharmaceutical composition comprising an excipient capable of binding water The invention concerns a solid pharmaceutical composition comprising less than 7% by weight of an oil or oily substance, a low dosage active ingredient, and a water insoluble non-cross-linked polymeric excipient capable of binding water and having a mean particle size greater than 150 µm. The composition can be obtained by a simple procedure comprising mixing the water insoluble non-cross-linked polymeric excipient capable of binding water and the active ingredient, which is dissolved or dispersed in an oil or an oily substance, in an aqueous dispersion thereof, or in water.
EP2194780A1 Method of treating glaucoma using rasagiline Disclosed is a method of reducing glaucoma in a subject afflicted with glaucoma, comprising administering to the subject an amount of R(+) -N-propargyl-1-aminoindan or a pharmaceutically acceptably salt thereof effective to reduce glaucoma.
CN102753563A Nucleoside analogs A purified compound having activity against hepatitis C virus is disclosed.
US8329637 Immunosuppression and antigen-specific immune tolerance; allogenic organ rejection, graft versus host disease, type I diabetes, rheumatoid arthritis, multiple sclerosis, systemic lupus erithematosus; chronic inflammatory disease; Crohn's disease and ulcerative colitis; asthma The invention discloses a combined preparation containing IL-10 and rapamycin, able to induce immunosuppression and antigen-specific immune tolerance, and the use thereof in the treatment of diseases involving an excessive, dysfunctional or uncontrolled immune responses mediated by T cells.
EP1532109A1 Pyrrolidine derivatives as oxytocin antagonists The present invention relates to novel pyrrolidine derivative of formula (I), its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein R1 is selected from the group comprising or consisting of H and C1-C6-alkyl, for the prevention and/or treatment of preterm labor, premature birth or dysmenorrhea.
US7160559 Galantamine hydrobromide particles and a water soluble film forming polymer are layered or coated on inert spheres, covered by a release rate controlling membrane made of a water insoluble polymer and optionally a plasticizer; galantamine and water-soluble polymer topcoat The present invention is concerned with controlled release compositions for oral administration comprising galantamine; and with processes of preparing such controlled release compositions.
CN101491519B Bilobalide injector and preparation method thereof The invention relates to the field of pharmaceutical preparations, in particular to a ginkgolides B injection and a preparation method thereof. The preparation method is characterized in that a mixed solvent of polyethylene glycol 600 and alcohol is added as a latent solvent. The ginkgolides B injection has steady quality, and cannot precipitate crystals after the long-term storage.
WO2012171479A1 Oxazolidinone compounds and their uses in preparation of antibiotics The invention belongs to the field of medicaments, in particular to oxazolidinone compounds and their uses in the preparation of antibiotics. The problem to be solved by the present invention is to provide new oxazolidinone compounds with structures shown as fomula (I). The oxazolidinone compounds of the present invention are new compounds obtained on the basis of a great amount of screenings and possess obvious antibacterial activity against bacteria such as drug-resistant staphylococcus aureus, fecal coliforms, streptococcus pneumoniae etc. and low toxicity, which are new choices for the development and application of antibiotics.
WO2011163085A3 Method and compositions use for endothelin-1 related kidney diseases The present application relates to methods of treating HIV-associated nephropathy (HIVAN) and/or focal segmental glomerulosclerosis (FSGS) using endothelin-1 (ET-1) antagonists. The application further relates to a composition for the treatment of HIVAN and/or FSGS. A kit for detecting the presence of ET-1 or ET-1 -associated biomarker in a biological sample is also disclosed.
WO2012009475A1 Methods of treating cancer with inhibition of lysine-specific demethylase 1 Disclosed herein are methods of treating cancer utilizing an inhibitor of lysine-specific demethylase 1 (LSDl), an LSDl inhibitor in combination with a DNA damaging agent or an inhibitor of poly (ADP-ribose) polymerase (PARP), or a histone deacetylase (HDAC) inhibitor in combination with a DNA damaging agent or a PARP inhibitor. In one embodiment, the methods include administering a therapeutically effective amount of an LSDl inhibitor to a subject with cancer (such as castration-resistant prostate cancer). In other embodiments, the methods include administering a therapeutically effective amount of an LSDl inhibitor and a therapeutically effective amount of a PARP inhibitor to a subject with cancer (such as prostate cancer, breast cancer, or ovarian cancer). In further embodiments, the disclosed methods include administering a therapeutically effective amount of an HDAC inhibitor and a therapeutically effective amount of a PARP inhibitor to a subject with cancer (such as prostate cancer, breast cancer, or ovarian cancer).
CN101390825A Intra-ocular release system of voriconazole The invention relates to a long-acting voriconazole intraocular medicine release system which contains voriconazole and is characterized in that the intraocular medicine release system also contains biodegradable medicinal high-molecular auxiliary material; voriconazole and biodegradable medicinal high-molecular auxiliary material are mixed to form homogenized mixture; the weight ratio of biodegradable high-molecular auxiliary material and voriconazole is 0.1:0.9-0.9-0.1; the molecular weight of the biodegradable high-molecular auxiliary material is 5000-1000000Dalton. The biodegradable high-molecular auxiliary material is selected from poly(lactide-co-glycolide) and polylactic acid. The release period of the voriconazole intraocular medicine release system is a week to a year, has less medicine dosage, less times of administration, reduces the adverse reaction caused by the repeated injection of vitreous cavity and greatly improve the compliance of patients; if the vitreous body base is implanted simultaneously during the excision operation of the central vitreous body, the complications of intraocular hemorrhage and retinal detachment caused by the repeated vitreous body puncture medicine-injection.
CN102993052A Aryl propionyl hydroxamic acid urease inhibitor, and synthesis and use thereof An aryl propionyl hydroxamic acid compound has the following structural general formula: The aryl propionyl hydroxamic acid compound has a good inhibiting effect for urease, and can be used to prepare drugs such as anti-gastritis drugs, anti-gastrohelcosis drugs and anti-lithangiuria durgs. The invention discloses a preparing method of the aryl propionyl hydroxamic acid compound.
EP1727801A1 Piperazines useful for treating pain Compounds of formulae (I) and (II) where Ar1, Ar2, R3, R4, and m, are disclosed herein, or a pharmaceutically acceptable salt thereof (a 'Nitro(cyano)vinylpiperazine Compound'); compositions comprising an effective amount of a Nitro(cyano)vinylpiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Nitro(cyano)vinylpiperazine Compound are disclosed.
US20080153792 Drug Identification and Treatment Method The invention relates to methods to identify compounds that can treat autoimmune conditions and treat specified clinical disorders such as multiple sclerosis, ulcerative colitis or arthritis. Compounds include 17α-ethynylandrost-5-ene-3β,15β,7α,17β-tetrol, 4α-acetoxy-17α-ethynylandrost-5-ene-3β,7β,17β-triol, 17α-ethynylandrost-5-ene-3β,4β,7α,17β-tetrol, 17α-ethynylandrost-5-ene-3α,4β,7α,17β-tetrol and 17α-ethynylandrost-5-ene-3α,4β,17β-triol-7-one.
US20070155663 Use of chemokine receptor agonists for stem cell transplantation A medicament comprising at least one agonist of receptors selected from the group consisting of the CCR3, CCR6 or CCR8 receptor or combinations thereof and a pharmaceutically acceptable carrier.
CN103386030A Drug for treating pediatric epilepsy The invention provides a drug for treating pediatric epilepsy. The drug comprises the following components in parts by weight: 4-8 parts of arisaema cum bile, 6-9 parts of tall gastrodia tuber, 6-12 parts of Indian bread, 15-20 parts of gambir plant, 7-12 parts of stiff silkworm, 8-12 parts of gypsum, 6-15 parts of sea-ear shell, 8-16 parts of grassleaf sweetflag rhizome, 6-15 parts of pearl powder and 9-12 parts of liquorice. The drug has the advantages and positive effects of obvious treatment effects, short treatment cycle and small side effects.
CN1823812A Formula of stable lentinan infiltration liquid and its preparation method A high-stability isotonic perfusion of leritinan and its preparing process are disclosed.
US20100130448 3',4',5-trimethoxy flavone derivatives as stimulatn of mucus secretion, method for the same, and pharmaceutical composition comprising the same The present invention provides a 3′,4′,5-trimethoxy flavone derivative and a pharmaceutically acceptable salt thereof, preparation thereof, and a pharmaceutical composition for the treatment and prevention of dry eye syndrome comprising the same as an active ingredient. The 3′,4′,5-trimethoxy flavone derivative and its pharmaceutically acceptable salt inhibit corneal damage through excellent stimulatory action on mucus secretion in the conjunctiva and therefore may be effective as a prophylactic or therapeutic agent for dry eye syndrome.
CN102511673A Coenzyme Q10 premix and its preparation method and use The invention discloses a coenzyme Q10 premix. The coenzyme Q10 premix belongs to the field of animal feed additives. The coenzyme Q10 premix comprises: by weight, 2 to 5% of coenzyme Q10 and 95 to 98% of carriers. The invention also discloses a preparation method of the coenzyme Q10 premix. The preparation method comprises that coenzyme Q10 and the carriers are mixed uniformly according to an equivalent incremental method. The invention also discloses a use of the coenzyme Q10 premix in improvement of pork quality, a pork color, production performances and a pork water-holding capacity and in reduction of a drip loss. The coenzyme Q10 premix can effectively improve pork quality and a pork color, improve a pork red value, reduce a pork yellow value, improve a pork water-holding capacity, and reduce a drip loss. In addition, the preparation method of the coenzyme Q10 premix is simple, has a low cost and is convenient for use.
EP1274473B2 Antimicrobial bioabsorbable materials The invention provides bioabsorbable materials with antimicrobial coatings or powders which provide an effective and sustainable antimicrobial effect. Specifically, this invention provides bioabsorbable materials comprising a bioabsorbable substrate associated with one or more antimicrobial metals being in a crystalline form characterized by sufficient atomic disorder, such that the bioabsorbable material in contact with an alcohol or water based electrolyte, releases atoms, ion, molecules, or clusters of at least one antimicrobial metal at a concentration sufficient to provide an antimicrobial effect. The one or more antimicrobial metals do not interfere with the bioabsorption of the bioabsorbable material, and do not leave behind particulates lager than 2 νm, as measured 24 hours after the bioabsorbable material has disappeared. Most preferably, the particulate sizing from the coating or powder is sub-micron, that is less than about 1 νm, as measured 24 hours after the bioabsorbable material has disappeared. Particulates are thus sized to avoid deleterious immune responses or toxic effects. Such antimicrobial metals are in the form of a continuous or discontinuous coating, a powder, or a coating on a bioabsorbable powder.
CN103263404A Composite anaesthetic The invention discloses a novel clinical composite anaesthetic. The anaesthetic is an injection or powder using an anti-oxidant and a conventional clinical anaesthetic as active components. According to the invention, combined usage of the anti-oxidant and the conventional clinical anaesthetic can substantially decrease a desired clinical dosage during individual usage of the conventional clinical anaesthetic without influencing anesthetic effects, so side effects of the anaesthetic, especially damage of the anaesthetic to important internal organs like the brain, the heart and the kidney, are reduced, the problems of a great usage amount and great side effects of the conventional clinical anaesthetic are overcome, discomfort of a patient in the process of treatment can be substantially reduced, and the risk of cognitive disorder of the patient caused by usage of a great amount of the anaesthetic is lowered down. The composite anaesthetic provided by the invention has the advantages of a small usage amount, safety and high efficiency and is applicable to clinical anesthesia induction and (or) maintenance of medication related to anesthesia induction of an operation and anaesthesia in an operation.
CN101601815A Medicament for hemostasis The invention discloses a medicament for hemostasis, being composed of pseudo-ginseng, ginseng fibrous root carbon, plant soot, Japanese beauty-berry, peanut skin, herba selaginellae moellendorfii, sangusis draconis, bletilla striata, fossilizid, carbonized pollen typhae and borneol. The invention has the advantages of no side effect, no irritation and obvious effect on hemostasis, the effective rate is 100%, the cure rate is above 99.9%, and no scars are left after curing.
CN1580062A Method for extracting total aglycone of Macrotys and its antitumour action The invention refers to the general glycoside of the overground part of Xing'an's bugbane rhizome and its application to the oxidation resisting damnification in the tumour treatment and tumour prevention. The so-called general glycoside is produced by the following steps: smash the the overground part of bugbane rhizome, screen it, distill it with 80% ethanol after refluence, filtrate it, condense it with lower pressure, add adsorbent (silica gel or diatomite) for column chromatography, get rid of the lipin with industrial caproylhydride first, wash it with ethyl acetate and condense part of the ethyl acetate with lower pressure and get the general glycoside. The invention is featured by simple technique, increased yield and low cost and has great potential of industrial production. And according to the result of the pharmacodynamics experiments, the general glycoside is hopefully used to produce the medicines of the chemical tumor prevention and treatment.
CN101157683A Sulfatase inhibiting agent The invention relates to sulfamic acid benzothiophene ester compounds with the formula of (Ia) or (Ib), wherein, R1, R2, R'2, R3, m and n are defined as in the specification. The invention also relates to pharmaceutical compositions containing the compounds and the using methods.
WO2007009757A1 Purine derivatives as agonists of the adenosine a2a receptor The invention relates to novel adenosine receptor agonists of formula (I), methods for their manufacture and their use as medicaments.
US20080113968 Substituted piperazines and diazepanes A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
WO2010096854A1 Methods of modulating the activity of the mc3 and/or mc4 receptors and treatment of conditions related to these receptors The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-3 receptor (MC3R) and / or the melanocortin-4 receptor (MC4R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC3R and / or MC4R is beneficial. Such diseases and/or conditions include, but are not limited to, obesity, eating disorders (such as cachexia, anorexia, weight gain, weight loss), metabolic syndrome, diabetes, sexual dysfunction (such as erectile dysfunction and female sexual dysfunction), anxiety, depression, inflammation, addiction and alcohol intake.
WO2012172635A1 Method for producing anticariogenic composition The purpose of the present invention is to provide a low-cost, high-efficiency production method which can produce a cyclodextran-containing composition that has the effect of inhibiting the formation of water-insoluble glucans and exhibits low acid productivity. The production method comprises: allowing a cyclodextran synthase to act on a dextran-containing culture medium to produce a cyclodextran-containing solution; and treating the resultant cyclodextran-containing solution using a nanofiltration membrane (an NF membrane) having a molecular weight cut-off of 400-800 daltons.
CN101531637A A novel compound capable of restraining and blocking M2 ion channel activity and application thereof The invention discloses a compound of formula (I) capable of restraining and blocking M2 ion channel activity or its pharmaceutical acceptable salts or stereo isomers. The compound or its pharmaceutical acceptable salts or stereo isomers can restrain and block wild-type and variant influenza and avian influenza M2 ion channel activity through a novel action mechanism, thereby having the pharmaceutical function for treating wild-type and variant influenza and avian influenza; and simultaneously they can also used for treating hepatitis B, hepatitis C and AIDS, so as to provide more drug choices for clinical treatment.
WO2007091165A1 A pharmaceutical composition comprising oenothein c useful for the treatment of peptic ulcer diseases The present invention deals with the pharmaceutical composition comprising the therapeutically effective amount of a compound oenothein C obtained from the bioactive fraction of plant Woodfordia fruticosa optionally along with one or more pharmaceutically acceptable carriers, additives, lubricants and diluents. Further it also provides a method of treating peptic ulcer diseases in a subject using the said pharmaceutical composition. It also relates to the use of the compound oenothein C in the treatment of peptic ulcer related diseases and a process for the isolation of the said compound.
US20080039366 Administering insulin, sodium citrate and phospholipid to respiratory tract The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a therapeutic, prophylactic or diagnostic agent or any combination thereof in association with a charged lipid, wherein the charged lipid has an overall net charge which is opposite to that of the agent upon association with the agent. Release of the agent from the administered particles occurs in a sustained fashion.
EP1503761A1 Substituted piperazines as melanocortin receptor ligands Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3a, R3b, R4a, R4b, R5, R7a, R7b, q, r, X, Y1, Y2, Y3 and Y4 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
CN102670622A Pharmaceutical composition containing bifonazole for treating superficial mycosis The invention provides a pharmaceutical composition for treating superficial mycosis. The composition contains bifonazole capable of resisting superficial mycosis and triamcinolone acetonide acetate with anti-inflammatory, anti-allergic and antipruritic effects.
US20090291152 Dibenzothiazepine derivatives This invention relates to novel 11-[4-[2-(2-Hydroxyethoxy)ethyl]piperazin-1-yl]dibenzo[b,f][1,4]thiazepine derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antagonists of seratonergic 5HT1A and 5HT2 receptors, dopaminergic D1 and D2 receptor, histaminergic H1 receptors, and/or adrenergic α1 and α2 receptors.
CN102225914B 3-alkenyl-4-aldehyde-5-aryl-4-isoxazoline compound, preparation method thereof and purpose thereof The invention relates to a 3-alkenyl-4-aldehyde-5-aryl-4-isoxazoline compound, a preparation method thereof and a purpose of the compound as an anti-tumor drug. The structural formula of the compound is shown in the specification, wherein R<1> is hydrogen, C1-4 alkyl or C2-5 alkenyl, R<2> is hydrogen, halogen, hydroxyl, nitrile, sulfonyl, nitro, or C1-4 alkyl or alkyloxy, R<3> is hydrogen, halogen, or C1-4 alkyl or alkyloxy, and R<4> is hydrogen, halogen, or C1-4 alkyl or alkyloxy. The 3-alkenyl-4-aldehyde-5-aryl-4-isoxazoline compound of the invention can be used to prepare antitumor drugs. The compound provided by the present invention has the advantages of high inhibition activity on the growth of tumor cells, simple preparation process and easy industrialization.
US20080070949 Polymorphs of rimonabant Crystalline form C of rimonabant and amorphous rimonabant, processes for their preparation and pharmaceutical compositions thereof.
EP1789404B1 Substituted n-arylsulfonylheterocyclic amines as gamma-secretase inhibitors This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R6)-, -S-, -S(O)-, or -S(O2)-; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, -C(O)-Y, -X-C(O)-Y, -alkylene-X-C(O)-Y, -alkylene-C(O)-Y, -alkylene-cycloalkylene-X-C(O)-Y, -alkylene-cycloalkylene-C(O)-Y, -cycloalkylene-alkylene-X-C(O)-Y, -cycloalkylene-alkylene-C(O)-Y, -cycloalkylene-X-C(O)-Y, -cycloalkylene-C(O)-Y, -alkylene-cycloalkylene-alkylene-X-C(O)-Y, -alkylene-cycloalkylene-alkylene-C(O)-Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR8R9, -N(R6)-(CH2)b-NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of Formula II and Formula III: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
CN102716118A Application of genistein and derivatives thereof in preparing hypnotic drugs The invention belongs to the field of compound drugs, relating to a new medicinal application of a compound genistein and derivatives thereof, in particular to the application of the genistein and the derivatives thereof in preparing hypnotic drugs and health products. The results of animal experiments for the genistein and the derivatives thereof show that the genistein and the derivatives thereof can cure insomnia by increasing non-rapid eyes movement sleeping time with an increase of about 80% in NREM sleep time within 6 hours after the animals being dosed. Especially, the NREM sleep time within 6 hours after the animals being dosed can be dosage-dependently increased. The genistein and the derivatives thereof have hypnotic activity and sleep quality improving effect, and can be used for preparing hypnotic drugs promoting sleep and drugs or health products improving sleep quality, especially suitable for treatment of sleep disorder in perimenopausal women.
WO2006120567A2 Pharmaceutical composition comprising an anti-bacterial agent and an active ingredient selected from carveol, thymol, eugenol, borneol and carvacrol The invention relates to a pharmaceutical composition comprising at least one first active therapeutic substance selected among carveol, thymol, eugenol, borneol, carvacrol, alpha-ionone, beta-ionone, as well as isomers, derivatives and mixtures thereof, and comprising at least one second active therapeutic substance that is an antibiotic.
CA2225761C Difluoroprostaglandin derivatives and their use A fluorine-containing prostaglandin derivative of the formula (1) (or a salt thereof) and a medicine containing it, particularly, a preventive or therapeutic medicine for an eye disease:
CN102532104A Novel aporphinoid compound and preparation method and application thereof The invention relates to a novel aporphinoid compound, a preparation method of the aporphinoid compound, medicine composition and important intermediate and application of the compound, in particular to a novel aporphinoid compound, stereoisomer of the aporphinoid compound, salt capable of being accepted in pharmacy or solvate capable of being accepted in pharmacy, the preparation method of aporphinoid compound, the medicine composition, the intermediate and application of the aporphinoid compound in preparation of medicine for protecting nerves in treatment of central nervous system diseases. The central nervous system diseases include Parkinson's disease, dementia praecox, depression, drug addiction and the like. The invention further relates to the preparation method of a compound of a general formula I, the important intermediate of the compound and application of the compound. Formula I is described as followed.
WO2005073220A1 Remedy for irritable bowel syndrome with diarrhea Use of 0.002 to 0.02 mg, in terms of daily dose, of ramosetron hydrochloride or an equimolar amount of ramosetron or a pharmaceutically acceptable salt thereof in order to produce a remedy for irritable bowel syndrome with diarrhea in male and female patients.
US7504408 Quinzoline derivatives for use in the treatment of cancer The invention concerns quinazoline derivatives of Formula (I) wherein each of Z, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.
US20090074721 Methods for treating viral infection with oral or injectibel drug solution Pharmaceutical composition comprising compounds and/or compositions useful to inhibit viral replication are disclosed.
US7786174 Administering a compound that inhibits islet amyloid polypeptide-associated amyloid deposition, e.g., 8-hydroxy-5-quinolinesulfonic acid, sodium cyclohexylsulfamate, or octahydroisoquinolinyl-N-propanesulfonic acid; antidiabetic agents Methods and compositions which are useful in the treatment of amyloidosis. In particular, methods and compositions are provided for inhibiting, preventing and treating amyloid deposition, e.g., in pancreatic islets, wherein the amyloidotic deposits are islet amyloid polypeptide (IAPP)-associated amyloid deposition or deposits. The methods of the invention involve administering to a subject a therapeutic compound which inhibits IAPP-associated amyloid deposits. Accordingly, the compositions and methods of the invention are useful for inhibiting IAPP-associated amyloidosis in disorders in which such amyloid deposition occurs, such as diabetes.
WO2004080450A3 Combined use of a fibrate and orlistat for the treatment of obesity The present invention relates to the use of a fibrate and orlistat to treat patients suffering from obesity.
WO2008028347A1 Combined antibiotics preparation A combined antibiotics preparation comprising piperacillin, sulbactam or clavulanic acid, ion chelants and/or buffers, which can be used to prepare a stable solution preparation, and can be used to prepare a stable solution preparation together with aminoglycoside antibiotics in one container.
EP1272187B1 Dopamine-d3 receptor ligands for the treatment of addiction The invention relates to the use of at least one compound of the general formula (I): L - D - B - G, wherein L and G represent aromatic, optionally heterocyclic groups, D is an aliphatic or heteroaliphatic link, and B is a 6-, 7- or 8-membered, saturated or unsaturated ring, bound via the 1 position to D and via the 4 or 5 position to G, and having one or two nitrogen heteroatoms, for treating disorders of the central nervous system, and especially for treating psychiatric or neurological disorders. The inventive compounds are especially useful in drug therapy.
US20100009920 Ttk as tumor marker and therapeutic target for lung cancer Disclosed herein is a method for determining kinase activity of TTK for EGFR and methods of screening for modulators of this kinase activity. Also disclosed are methods and pharmaceutical compositions for preventing and/or treating lung cancer that use or include such modulators. Methods for diagnosing lung cancer using the kinase activity of TTK for EGFR protein as an index as well as methods for assessing and prognosing lung cancer are also provided.
CN102438634A A composition comprising silver nanoparticles and extracts of polygonum multiflorum thunb and the use thereof A pharmaceutical composition comprising effective amount of silver nanoparticles and extracts of Polygonum Multiforum Thunb, a method for increasing hair growth by administering the said pharmaceutical composition locally to a host, and use thereof are disclosed.
US20120283234 Bile Acid Derivatives As FXR Ligands For The Prevention Or Treatment Of FXR-Mediated Diseases Or Conditions The present invention relates to compounds of formula (I): wherein R is hydrogen or alpha-hydroxy, the hydroxyl group in position 7 is in the alpha or beta position; and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.
US7632850 2-amino-2-oxoethyl 1-(4'-fluoro-1,1'-biphenyl-4-yl)cyclopropylmethylcarbamate and 2-(methylamino)-2-oxoethyl 1-(4'-fluoro-1,1'-biphenyl-4-yl)cyclopropylmethylcarbamate; fatty acid amide (FAAH) hyrdrolase inhibitors; analgesics; neuropathic pain;psychological disorders; anticarcinogenic agents; AIDS The present invention provides a compound of the formula (I): in which R1, R2, R3, A and n are described and set forth more fully herein. Also provided are their preparation and their application in therapy.
EP2605764A1 Combination anti - cancer therapy The present invention relates to a combination therapy of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor for treating a patient suffering from a proliferative disorder, in particular a solid tumor, for example, colorectal cancer, melanoma, and thyroid cancer.
CA2833633A1 Composition and method for enhancing an immune response Disclosed are methods and compositions for treating or preventing microbial infections.
US20080153857 Specific capsaicin receptor modulators; analgesics; neuropathic pain; obesity; antitussives, hiccups; e.g. (4-Cyclopropyl-phenyl)-[2-methoxymethyl-7-(3-trifluoromethyl-pyridin-2-yl)-quinazolin-4-yl]-amine Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
US20050208040 Polynucleotides and polypeptides encoded thereby The invention provides polypeptides, designated herein as PROX polypeptides, as well as polynucleotides encoding PROX polypeptides, and antibodies that immunospecifically-bind to PROX polypeptide or polynucleotide, or derivatives, variants, mutants, or fragments thereof. The invention additionally provides methods in which the PROX polypeptide, polynucleotide, and antibody are used in the detection, prevention, and treatment of a broad range of pathological states.
US20080312171 Tetracycline-Dependent Regulation of Rna Interference The present invention relates to a tetracycline dependent gene regulatory system or composition controlling the expression of a target gene in a cell and to methods using said system or composition. The present invention more specifically discloses compositions, vectors and methods allowing tetracycline-controlled expression of short-hairpin RNAs (shRNAs), and demonstrates inducible, reversible and stable RNA interference (RNAi) using the same in a cell. The invention can be used to cause reversible control of the expression of any gene and may therefore find applications in the fields of mammalian, in particular human, genetics and molecular therapeutics, in cell and gene therapy, research as well as in genetic studies using transgenic animals.
WO2007075102A1 Medicinal agent for treating viral infections The invention relates to medicine, in particular to searching and developing novel medicinal agents for treating and preventing viral infections, mainly influenza viruses. The aim of said invention is to develop more efficient and low toxic medicinal agents by combining arbidol and the analogs thereof with a preparation exhibiting another mechanism of action. Said combinations enhances the efficiency of the preparation small doses and makes it possible to reduce the probability of side effects and appearance of virus resistant strain by reducing the dose. The result is attained by the combined use of arbidol and the analogies thereof with at least one type of preparation selected from the following group of antiviral preparations: ribavirin, zanamivirin, oseltavirin, peramirin, amantadin or remantadin.
WO2010135972A1 Preparation methods and uses of 1-(substituted aryl)-5-trifluoromethyl-2-(1h)-pyridone compounds and their salts A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)-pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.
CN102342924A Medicine composition containing agomelatine The invention belongs to the technical field of medicine, and discloses a medicine composition containing agomelatine prepared form components of, by weight: 11% to 25% of agomelatine, 30% to 65% of lactose, 11% to 40% of starch, 8% to 15% of carboxymethylstarch sodium, 0.5 to 5% of stearic acid, 0.6% to 2% of magnesium stearate, and 0.5% to 5% of silicon dioxide. As a result of experiments, preparations prepared with the medicine composition provided by the invention provide a better dissolution rate.
US20130281917 Carbon dioxide, saline and additional active nasal delivery methods and treatments Methods for treating ailments in a patient in need thereof includes the step of directing a therapeutic, non-inhaled dosage to at least one nasal cavity of the patient through a flow regulating device while the patient refrains from inhaling. The dosage includes (a) a saline fluid (b) a gas containing carbon dioxide and (c) at least one additional active component, wherein the therapeutic, non-inhaled dosage is delivered at a flow rate from 1 cc/sec to 20 cc/sec for a duration of 2 to 30 seconds.
US6951882 treating obesity or a sleep/wake disorder mediated by orexin-2; antagonists Urea-containing, substituted 4-phenyl-[1,3]-dioxanes, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, obesity or a sleep/wake disorder mediated by orexin-2 are described.
CN103142523A Dropping pills containing etoposide The invention relates to dropping pills, and in particular to dropping pills containing etoposide clathrate compounds.
CN103222956A Strychnine-hydroxypropyl-beta-cyclodextrin liposome, preparation method and applications thereof The present invention discloses a strychnine-hydroxypropyl-beta-cyclodextrin liposome, which contains, by weight, 0.5-2 parts of strychnine, 2-20 parts of a strychnine-HP-beta-cyclodextrin inclusion compound, 20-200 parts of soybean lecithin, and 5-20 parts of cholesterol. The present invention further discloses a strychnine-hydroxypropyl-beta-cyclodextrin liposome preparation method, which comprises: carrying out inclusion on strychnine with hydroxypropyl-beta-cyclodextrin, and then preparing into the liposome. According to the present invention, drug loading capacity is improved, an elimination half-life of the strychnine is prolonged, stability is improved, lymphatic system targeting is achieved, toxic and side effects on heart and central nervous system are reduced, and bioavailability is improved.
US20100137348 Pharmaceutical formulations: salts of 8-[-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
CN101716149A New precursor medicinal preparation The invention discloses a freeze-drying preparation of a water-solubility propofol precursor compound and a preparation method thereof. The freeze-drying preparation of the propofol precursor compound, prepared in the method of the invention, has the advantages of favorable water solubility, stability and safety.
US20110262369 Crystalline, enantiomerically pure salt form of a beta-agonist, and the use thereof as a drug The invention relates to a crystalline, enantiomerically pure hydrochloride salt of N-(5-{2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino]-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methane sulfonamide, preferably N-(5-{(R)-2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino]-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methane sulfonamide, and the effect thereof as a long-term betamimetic agent, alone or combined with at least one other active ingredient, in the treatment of respiratory diseases.
CN101984973A Medicinal application of 20(R)-25-methoxyl-dammarane-3 beta,12 beta,20-triol The invention belongs to the technical field of medicines, relating to a medicinal application of a compound, namely 20(R)-25-methoxyl-dammarane-3 beta,12 beta,20-triol (25Rmdt for short). The 25Rmdt has the antitumor activities of inhibiting the growth and proliferation of various oncocytes, inducing the differentiation and apoptosis of cancer cells, inhibiting tumor angiogenesis, restraining the infiltration and proliferation of the tumors, enhancing immunity of the organism, reducing the toxic and side effect of chemotherapeutics and the like, and is mainly applied to the prevention and treatment of malignant tumors, and the total effective dose of the 25Rmdt is 1-100mg/kg/d.
US8658673 BETA2-adrenoreceptor agonists Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.
WO2009063991A1 Pyridooxazepine derivative and use thereof Disclosed is a compound represented by the formula below, which has excellent serotonin 5-HT2C receptor activating activity. Specifically disclosed is a compound represented by the formula below or a salt thereof. (In the formula, A represents -OR1 or -S(O)pR2; R1 and R2 each represent a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group; and p represents 0, 1 or 2.)
EP1841767A1 Pyrazolopyridines, their preparation and their medical use The invention relates to pyrazolopyridines according to the general formula (I), and salts thereof, to pharmaceutical compositions comprising said pyrazolopyridines and to a method of preparing said pyrazolopyridines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with angiopoietin and therefore influence Tie2 signalling.
US20090105259 Acyclic 1,4-Diamines and Uses Thereof This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain acyclic diamines, which are agonists of TRPV4 channel receptors.
CN102898538A Abalone viscera acidic polysaccharose and health-care product containing abalone viscera acidic polysaccharose and application of abalone viscera acidic polysaccharose The invention provides abalone viscera acidic polysaccharose. According to the abalone viscera acidic polysaccharose, a main chain comprises rhamnose and glucuronic acid, wherein a C-2 position or C-3 position of the rhamnose in the main chain is subjected to sulphating; and the rhamnose in the main chain is connected with the rhamnose or galactose to form a branched chain structure. The abalone viscera acidic polysaccharose which is extracted from abalone viscera can promote the proliferation of hepatoma carcinoma cells (HepG2) in vitro obviously, and has a certain effect of dose dependency; and experiments of studying a repair effect of the abalone viscera acidic polysaccharose on the HepG2 cells which are subjected to oxidative damage and on rat hepatic tissues which are subjected to acute hepatic damage caused by carbon tetrachloride in vivo indicate that the abalone viscera acidic polysaccharose can be used as a functional factor for protecting liver.
US7947682 Substituted N′-pyrrolo[1,2-a]quinoxalin-4-yl-hydrazides as anti-cancer agents Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Such compounds include a compound of Formula II, wherein R is H, alkyl, or halogen; R′ is H, alkyl, or halogen; X is CH or N; and Y comprises a homocyclic or heterocyclic ring. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating gene expression.
WO2009121219A1 An use of arsenide for the preparation of antiviral drugs An use of arsenide for the preparation of antiviral drugs which can solve problems such as expensive therapy,sequela etc. Arsenide is one of As2S2,As2S3,As4S4,As2O3, and As3S3,it can destroy all kinds of protein enzyme dissolvingly and inactivate the enzyme. As a result, it will prevent virus's duplication in vivo and have antiviral effect.
CN1948315A Tricycle compounds and its application in making medicine The present invention relates to a tricyclic compound or its stereo-isomer or its pharmaceutically-acceptable salt and their application in preparation of medicine for curing the disease of central nervous system. Besides, said invention also provides the chemical general formula of said tricyclic compound and its detailed description.
WO2006072351A1 Heteroaryl-substituited pyrazolines as par-1 antagonists The invention relates to the field of blood coagulation and, in particular, to the use of heteroaryl-substituted pyrazolines as medicaments, novel heteroaryl-substituted pyrazolines and to methods for the production thereof, in addition to the use thereof for producing medicaments for treating and/or for the prophylaxis of illnesses, in particular cardiovascular diseases, preferably thromboembolic diseases.
CN101485674B Application of naringin in preparing anti-depression medicament The invention discloses application of naringin in preparation of an anti-depression medicine. Dosage forms of the medicine are pharmaceutically acceptable dosage forms such as a tablet, a capsule, a solution, a suspension, an injection, a dripping injection and the like. A composition consists of the naringin as well as aglycon and secondary glucoside which are pharmaceutically acceptable and are generated through hydrolysis or enzymolysis, and is combined with pharmaceutical carriers to prepare various pharmaceutical dosage forms. The medicine has small toxicity, and overcomes the disadvantages of the prior anti-depression medicines such as excitation, constipation, anuresis, dizziness, hypersomnia, tremor and the like.
US7553821 Methods for selectively modulating survivin apoptosis pathways The present invention, based on the discovery of a new biological phenomena, provides methods and compositions for use in identifying agents that modulate the phosphorylation of survivin, the interaction between survivin and p34cdc2-cyclin B1 kinase complex, and the interaction between survivin and caspase-9. Related methods and compositions can be used to modulate survivin regulated apoptosis.
US20110200693 Increasing the efficiency of utilization of ingested creatine The present invention generally relates to increasing the efficiency of usage of an ingested exogenous biologically active substance by a body. In particular, the present invention relates to ways to improve the efficiency of utilization of ingested creatine in a body, in particular to increase the storage of creatine in the body. One embodiment of the present invention is the use of a combination comprising creatine and a soluble fiber for the preparation of a composition to increase the storage of creatine in the body.
EP2665732A1 Fused aminodihydrothiazine derivatives useful as bace inhibitors The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or -C≡N; and pharmaceutically acceptable salts thereof; which compound has an Αβ production inhibitory effect or a BACEl inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Αβ and typified by Alzheimer-type dementia.
WO2011159693A2 Oral treatment of digital ischemic lesions Provided are methods of orally treating ischemic diseases and conditions, such as digital ulcers, associated with or caused by the ischemic diseases.
US20110313042 Amino Acid Compositions An amino acid composition is disclosed. The composition includes: at least one constituent selected from the group consisting of a nitrate, a nitrite, and both; and at least one constituent amino acid selected from the group consisting of Arginine, Agmatine, Beta Alanine, Citrulline, Creatine, Glutamine, L-Histidine, Isoleucine, Leucine, Norvaline, Ornithine, Valine, Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, and Phenylalanine Also disclosed are a method for increasing the bioabsorption of Amino Acids in a human or animal and a method for increasing vasodilative characteristics of Amino Acids in a human or animal.
CN101361746A Stable adriablastina albumin lipid drug-loading system and preparation method thereof The invention discloses a stable system for carrying adriamycin albumin lipid and a preparation method thereof. The invention is characterized by combining the adriamycin on albumin lipid vesica through ultrasonic, high pressure isotrope or micro-fluidization technique. The invention has the advantages of both significantly improving the efficacy and stability of adriamycin lipid vesica and raising the entrapment rate of medicine in the lipid vesica.
US20090270440 Bioavailability of active substances having an amidine function in medicaments The invention relates to the use of N,N′-dihydroxyamidine (I), N,N′-dihydroxyamidine ether (II), N,N′-dihydroxyamidine diether (III), N,N′-dihydroxyamidine ester (IV), N,N′-dihydroxyamidine diester (V) or 4-hydroxy-1,2,4-oxadiazoline (VI) of the formulae cited above, wherein R represents hydrogen, an alkyl and/or aryl radical, as a substitute for an amidine function of a medicament for improving the bioavailability of the medicament.
CN103284953A Bicyclol solid preparation and preparation method thereof The invention discloses a bicyclol solid preparation and a preparation method of the bicyclol solid preparation. Because the bicyclol is a slightly soluble drug, the bicyclol is treated by adopting a micronization mode, and the particle size is reduced. The main drug bicyclol, a filling agent and a solubilizer are combined, ground and micronized, the micronization difficulty is reduced, the dissolution effect is good, the bioavailability is high, and the bicyclol solid preparation is simple and convenient in operation and stable in process.
CN102755348A Carbohydrate and electrolyte injection and preparation method thereof The invention provides a carbohydrate and electrolyte injection which comprises the following components by weight part: 30 parts of glucose, 15 parts of fructose, 7.5 parts of xylitol, 0.73 part of sodium chloride, 0.41 part of sodium acetate, 0.185 part of calcium chloride, 0.255 part of magnesium chloride, 0.87 part of dipotassium phosphate, 0.0007 part of zinc sulfate, 0.21 part of sodium bisulfite and 250 parts of water for injection; and the PH value is 5.1-5.5. The injection is low in cost and wide in applicable range. The invention also provides a preparation method of the carbohydrate and electrolyte injection. The preparation method comprises the steps of dissolving carbohydrate and electrolyte (as raw and auxiliary materials), absorbing, decarbonizing, adjusting the pH, and sterilizing to obtain the carbohydrate and electrolyte injection. According to the preparation method, the process is simple, the method is suitable for industrial production, the problems that samples turn yellow after the sterilization, and white substances are separated out can be avoided by increasing the dissolving temperature to be 75 DEG C-85 DEG C and adjusting the pH of the solution, so thatthe carbohydrate and electrolyte injection is stable.
CN102108092A 23-hydroxy betulinic acid derivative as well as preparation method and application thereof The invention discloses a 23-hydroxy betulinic acid derivative as well as a preparation method and application thereof. The derivative has a structure as shown in a formula (I). The 23-hydroxy betulinic acid derivative can be used for resisting tumors and used as a tumor medicament resistance reversal agent. The 23-hydroxy betulinic acid derivative can be used for effectively inhibiting the proliferation of tumor cells and also can be used for obviously increasing the antipersonnel force of DOX (doxorubicin) on a P-glycoprotein overexpression cell strain HepG2/ADM under the condition of non-toxicity dosage.
WO2014050144A1 Dentinal tubule blocking agent Provided is a dentinal tubule blocking agent including a calcium-containing component, the calcium-containing component being (i) a phosphorylated saccharide calcium salt, (ii) a combination of a phosphorylated saccharide salt other than a phosphorylated saccharide calcium salt or a phosphorylated saccharide and a calcium salt other than a phosphorylated saccharide calcium salt or (iii) a mixture of (i) and (ii), and the phosphorylated saccharide being composed of a saccharide moiety and a phosphate group. The dentinal tubule blocking agent may either contain 0.1 weight% or more of hydroxyapatite, or not contain hydroxyapatite or contain less than 0.1 weight% of hydroxyapatite.
CN102603738B Stable moxifloxacin hydrochloride compound The invention discloses a stable moxifloxacin hydrochloride compound. The moxifloxacin hydrochloride compound provided by the invention is prepared through the steps that: moxifloxacin hydrochloride is heated and dissolved in an ethanol-acetonitrile-water solution; proper amounts of potassium nitrate and hydrochloric acid are added to the solution; the pH value is regulated; the solution is stirred, and is washed by using ethanol; the solution is dried, such that the stable moxifloxacin hydrochloride compound is obtained. The stability of the moxifloxacin hydrochloride compound provided by the invention is good, and the compound is convenient to produce, transport, and store. A production technological process is short, the product yield is high, and the production cost is low. Therefore, industrialization can easily be realized.
US20100130619 Pharmaceutical composition for parenteral administration of idebenone The invention describes use of an injectable form of Idebenone, suitable for intravenous injection or infusion. The proposed formulation is an oil-in-water emulsion, where Idebenone is associated with the oil droplets.
DE102006030366A1 Pharmaceutical composition useful for treating Parkinson's disease comprises a substance that specifically interacts with a homer1 gene Pharmaceutical composition comprises a substance that specifically interacts with a homer1 gene, with a regulatory protein of a homer1 gene, with a homer1 gene product or with a component of a signal transduction pathway comprising a homer1 gene or its gene product. An independent claim is also included for screening for substances that reduce the symptoms of Parkinson's disease by providing a group of nonhuman organisms that have symptoms of Parkinson's disease and express a homer1 protein, administering test substances to part of the group, comparing the symptoms of treated and untreated organisms, and detecting the specific interaction of the substances with a homer1 gene, with a regulatory protein of a homer1 gene, with a homer1 gene product or with a component of a signal transduction pathway comprising a homer1 gene or its gene product. - ACTIVITY : Antiparkinsonian. No biological data given. - MECHANISM OF ACTION : Homer1 gene inhibitor.
WO2014059499A1 Preparation method and composition of a pharmaceutical drug from quenodeoxicholate linked to a natural, d-fructose-analogue, sulfamate-derived monosaccharide (topiramate) and to a phenylketone (bupropion) for the treatment of obesity and plurimetabolic syndromes The invention, preparation method and composition of a pharmaceutical drug from quenodeoxicholate linked to a natural, d-fructose-analogue, sulfamate-derived monosaccharide (topiramate) and to a phenyl ketone (bupropion) for the treatment of obesity and plurimetabolic syndromes, essentially consists of a new chemical entity having a specific receptor in the biological membrane that improves absorption due to the active transport thereof, which molecule releases, after being hydrolysed, bupropion and topiramate, which have already been shown to be effective for the treatment of obesity and plurimetabolic syndromes. Bupropion is an aminoketone which has, as mechanism of action, a slight norepinephrine, serotonin and dopamine reuptake inhibition effect and which has been shown to promote weight loss in various studies, with low incidence of adverse events. Topiramate is a sulfamate-substituted, 1,6-diphosphate fructose analogue that induces weight loss, human studies suggesting that it plays a role in the decrease of calorie ingestion, and in hormone involvement in obesity and glucose and lipid metabolism. A new chemical entity associating the molecules of these two pharmaceutical drugs achieves a synergistic effect, since each part acts on a particular physiological system to reduce body weight in overweight or obese patients.
EP1165096B1 Use of cytidine derivatives for the treatment of leukaemia The present invention provides a novel method for treating leukemia and more particularly acute myelogenous leukemia (AML) in a host comprising administering to the host a therapeutically effective amount of a compound having formula (I): wherein B is cytosine or 5-fluorocytosine and R is selected from the group comprising H, monophosphate, diphosphate, triphosphate, carbonyl substituted with a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, and (a) wherein each Rc is independently selected from the group comprising H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and an hydroxy protecting group; and wherein said compound is substantially in the form of the (-) enantiomer.
CN101367809A Penem derivant containing sulfhydryl pyrrolidine formhydrazide The present invention belongs to the technical field of medicine, in particular to a penem derivative containing mercaptopyrrolidine formylhydrazine shown in the formula (1) and a pharmaceutically acceptable salt, an easily hydrolyzed ester, an isomer, a hydrate and a hydrate of the ester or the salt thereof: wherein, R<1>, R<2>, R<3>, R<4>, R<5>, R<6> and X are defined in the description. The present invention also relates to preparation methods of the compounds, drug combinations and applications of the compounds in the preparation of drugs for treating and/or preventing infective diseases.
CN101983634A Liquid for treating marginal blepharitis The invention discloses a preparation method for a liquid for treating marginal blepharitis. The preparation method is realized by the following technical scheme: placing bear gall and cow gall in a refrigerating chamber with the temperature of minus 40 DEG C for 24h, taking out and completely melting the bear gall and the cow gall, filling white sugars in the bear gall and the cow gall respectively, bundling the bear gall and the cow gall tightly, soaking the bear gall and the cow gall in water for 24h, taking out the bear gall and the cow gall, evenly mixing the two types of gall, and filling the mixture in bottles to obtain the finished liquid. Users get well within short time if the liquids of the invention are used.
US20060040906 Piperazine urea derivatives as melanocortin-4 receptor agonists Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.
EP2548865A1 Novel bis-indolic derivatives, their uses in particular as antibacterials The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
CN102240268A Sustained/controlled release microsphere of biological extract Genipin cross-linked chitosan coated stilbene compound and preparation method thereof The invention discloses a sustained/controlled release microsphere of a chitosan coated stilbene compound using a biological extract Genipin as a cross-linking agent and a preparation method thereof. In the microsphere, a cross-linked condensation compound layer of the chitosan and the Genipin serves as a capsule shell and is used for coating a medicament 3,5-dihydroxyl-4-isopropyl stilbene, resveratrol, pterostilbene, oxidized resveratrol or piceatannol; the medicament stability of the product is improved; the sustained/controlled release of the medicament is realized; and the released Genipin after in vivo metabolism of the capsule shell has the characteristics of biocompatibility, no cytotoxicity and the like. The invention is applicable to the sustained/controlled release microspheresof Genipin cross-linked chitosan coated 3,5-dihydroxyl-4-isopropyl stilbene, resveratrol, pterostilbene, oxidized resveratrol, piceatannol and other stilbene compounds and a preparation method thereof. The preparation method is low in requirements on the control condition and easy to operate. In the microspheres, the quality is uniform; the grain size is 0.1 to 100 mu m; the surface of the microsphere has a multiporous structure; and the entrapment rate of the capsule shell to the medicament is 30 to 90 percent.
WO2006079910A3 0-(3-piperidino-2hydroxypropyl)nicotinic amixodime for treating lesions in the oral cavity The invention refers to the use of of 0-(3-piperidino-2hydroxypropyl)nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof for the preparation of a pharmaceutical composition or a mouth and tooth care composition suitable for the treatment of lesions in the oral cavity.
US20080075735 Demethylated and/or oxidized membrane DNA A process for the preparation of oxidized and/or demethylated antigens comprising the steps of treating a cell with a stress factor selected from the group consisting of UV-radiation, oxidizing reagents, heavy metal salts, drugs, nucleoside and nucleotide analogs, and enzyme inhibitors lyses of the cell to give a cell lysate purification of oxidized and/or demethylated antigens from the cell lysate.
US8133502 System for delivering a composition to the nasal membrane and method of using same A quick and easy system and method for delivering a composition to a nasal membrane is presented. The applicator assembly includes a sleeve member which encases a swab having a portion that contacts a gelled composition. The sleeve member is manually severed to expose the applicator and the composition. The gelled composition contained on the applicator is applied to the nasal membrane.
WO2010036799A1 Therapeutic regimen comprising peg- interferon, ribavirin and vx-950 for the treatment of hepatitis " The present invention relates to antiviral therapies and compositions for treating or preventing Hepatitis C infections in patients and relates to other methods disclosed herein. The invention also relates to kits and pharmaceutical packs comprising compositions and dosage forms.
CN103356544A Application of Sarcaboside B in monoamine oxidase inhibitor drug The invention provides application of Sarcaboside B in preparation of monoamine oxidase (MAO) inhibitor. Compared with the existing monoamine oxidase inhibitor, the inhibitory activity and the selecitivty for MAO-A and MAO-B of the monoamine oxidase inhibitor prepared by Sarcaboside B are greatly improved. The application of Sarcaboside B in preparation of monoamine oxidase (MAO) inhibitor is disclosed by the invention for the first time. As the skeleton type is brand new and Sarcaboside B has unexpectedly strong activity for inhibiting monoamine oxidase, the possibility that any enlightenments are given by other compounds does not exist. Sarcaboside B has prominent substantive features and has remarkable progress when being used for treating monoamine oxidase imbalance-associated diseases.
CA2164276C New highly selective process for the preparation of enantiomerically pure phenylsubstituted 1,4-dihydropyridine-3,5-dicarboxylic acid derivatives The present invention relates to a new highly selective process for the preparation of enantiomerically pure halogeno-phenyl-substituted 1,4-dihydropyridine-3,5- dicarboxylic esters of the general formula (I) (see formula I) in which R1 to R3 have the meanings given in the description.
WO2013167707A1 Composition for the treatment or prevention of urinary tract infections and dosage form The invention relates to a cranberry composition for the treatment or prevention of vaginal and urinary tract infections, and a dosage form for vaginal administration of such a composition. The composition comprises an a cranberry extract and optionally other active ingredients and/or excipients. Of particular interest are compositions for vaginal administration. When administered to the vagina, cranberry induces a p H normalizing effect which contributes to curing vaginal infections. A preferred embodiment comprises a combination of cranberry extract, lactitol and hyaluronic acid.
CN103271909A Human breast cancer therapeutic drug taking electric pressure controlled proton channel Hv1 as target spot Provided is a human breast cancer therapeutic drug taking an electric pressure controlled proton channel Hv1 as a target spot. The drug is lansoprazole, the other name is 2-[[3-Methyl-4-(2,2,2-trifluoroethoxy)pyridine-2-yl]methylsulfinyl]-1H-benzoimidazole, and the molecular formula is C16H14F3N3O2S. The human breast cancer therapeutic drug takes the electric pressure controlled proton channel Hv1 as the target spot, and the lansoprazole is a drug for treating the human breast cancer. The lansoprazole has certain inbibitional effect on the growth, migration and infiltration of the human breast cancer cell with a relatively high degree of malignization, therefore, the malignization provided by the invention can be used as the drug to treat the human breast cancer, and the prospect is very wide.
US20090061048 Delivery and controlled release of encapsulated lipophilic nutrients A complex coacervate delivery system is provided which encapsulates lipophilic nutrients such as, for example, fish oils high in omega-3 fatty acids. The complex coacervate delivery system protects the lipophilic nutrient from degradation, e.g., oxidation and hydrolysis, and also reduces or eliminates the unpleasant taste and odor of the lipophilic nutrient. The complex coacervate delivery system upon ingestion is operative to substantially release the lipophilic nutrient in the lower gastrointestinal tract in a pH-controlled manner. The complex coacervate delivery system may be included in a food or beverage product having a pH value within the range of about 1.5 to about 5.0.
US20120190634 Lipoteichoic acid-derived glycolipids, and compositions comprising same A lipoteichoic acid (LTA)-derived glycolipid, and a pharmaceutical, food or cosmetic composition and a vaccine adjuvant including the same are provided. The LTA-derived glycolipid can inhibit the production of inflammatory cytokines and thus have anti-inflammatory effects. Therefore, the pharmaceutical, food or cosmetic compositions including the LTA-derived glycolipid can be used to prevent and treat inflammatory diseases, and the LTA-derived glycolipid can be also used as the vaccine adjuvant.
CN1880343A Chemically modified polyaminosaccharide by a hydrocarbyl sultone compound This invention discloses chemically modified polyaminosaccharides, in particular chemically modified chitosans, in the molecular structure of which a predetermined proportion of the amino functional groups is sulfonated by the hydrocarbyl sultone compound via a covalent bond. Such chemically modified polyaminosaccharides may be produced by a process of sulfonating an un-modified polyaminosaccharide having amino functional groups by a hydrocarbyl sultone compound in the presence of an organic solvent under a suitable temperature. Chemically modified chitosans of this invention may be used in a variety of applications, including wound healing.
WO2006097220A1 Pyrimidine carboxylic acid derivatives and use thereof The invention relates to pyrimidine carboxylic acid derivatives of formula (I), to methods for the production thereof, to their use for treating and/or preventing diseases, and their use for producing medicaments for treating and/or preventing diseases, preferably for treating and/or preventing cardiovascular diseases, in particular, dyslipidemias and arteriosclerosis.
US7074821 Taxoids, their preparation and pharmaceutical composition containing them New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them. In general formula (I), Ar represents an aryl radical, R represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.
EP0830139B1 Modified myelin protein molecules Compositions and methods are provided for the clinical assessment, diagnosis, and treatment of multiple sclerosis. The compositions of the invention are molecules related to the human proteolipid protein (PLP) and/or human myelin basic protein (MBP), and include nucleic acids and polypeptides. The nucleic acid molecules of the invention are useful in the production of modified PLP polypeptides and modified MBP polypeptides, such polypeptides being useful for assaying T cells for responsiveness to PLP and MBP epitopes. The polypeptides of the invention are also useful as therapeutic agents that act by inducing T cell responses, including anergy and apoptosis, as a means of treating multiple sclerosis.
CN103251730A Granules for treating upper gastrointestinal hemorrhage and ulcer and preparation method thereof The invention discloses granules for treating upper gastrointestinal hemorrhage and ulcer, which are characterized in that the formula comprises 150 parts by weight of liquorice, 150 parts by weight of dried rehmannia, 150 parts by weight of bighead atractylodes rhizome, 150 parts by weight of monkshood, 150 parts by weight of donkey-hide gelatin, 150 parts by weight of scutellaria baicalensis, 250 parts by weight of furnace soil, 1-5 parts by weight of corrigent, and 100-150 parts by weight of forming agent. According to the invention, huangtu decoction is changed into granules (solid preparation); medicine stability is obviously increased; the granules are easy to store; granule medicine packaging is lower in error; the granules are packaged into bags according to dosage each time; and the granules disclosed by the invention are convenient for packaging and taking, accurate in dosage, safe and free from side effects.
US20130012539 Compositions and Methods for Treating Lysosomal Disorders The present invention provides compositions and methods for treating lysosomal disorders using a class of substituted imidazole derivatives or compounds.
CN102240272A Potassium citrate sustained release tablet and preparation method thereof The invention provides a potassium citrate sustained release tablet and a preparation method thereof. A weight ratio of potassium citrate to a waxy sustained release matrix is 10:0.7-1.1, preferably 10:0.83-1.0, and most preferably 10:1.0. The sustained release tablet allows the concentration of citric acid radical in urine to be effectively increased, the fluctuation of the concentration of citrate in the urine to be reduced, and a stable and high level of the citrate concentration to be kept. More importantly, the three-hour release rate, the tabletting performance and the moisture resistance of the sustained release tablet are further improved.
US20070249590 Substituted indolo[2,3-a]pyrrolo[3,4-c]carbazole compounds useful in treating kinase disorders The present invention is directed to substituted indolo[2,3-a]pyrrolo[3,4-c]carbazole compounds of formula (I): and forms thereof and their synthesis and use as protein kinase inhibitors and interactions thereof.
US20100028350 Preventing il-2 mediated inflammation in epithelial cells The present invention provides new methods for treating, minimizing and/or preventing inflammatory injury involving IL-2 activity on epithelial cells expressing IL-2 receptors. Methods for reducing or preventing inflammatory injury in a tissue/organ comprise inhibiting IL-2 receptor activity in cells of the tissue/organ.
WO2006137794A1 New2-azetidinone derivatives for the treatment of hyperlipidaemic diseases The invention relates to novel 2-azetidinone derivatives of formula (I) and to pharmaceutically acceptable salts, solvates and prodrugs thereof . The compounds are cholesterol absorption inhibitors, useful in the treatment of hyperlipidaemic conditions. The invention also relates to processes for their manufacture and to pharmaceutical compositions containing them.
US8853208 Amino alcohol-substituted arylthienopyrimidinones, process for their preparation and their use as medicaments The invention relates to amino alcohol-substituted arylthienopyrimidinones having a formula I and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one amino alcohol-substituted arylthienopyrimidinone of the invention or its derivative, and the use of the amino alcohol-substituted arylthienopyrimidinones of the invention and their derivatives as MCH antagonists.
WO2013113857A1 (1r,4r)-6'-fluoro-(n-methyl- or n,n-dimethyl-)-4-phenyl-4',9'-dihydro-3'h-spiro-[cyclohexane-1,1'-pyrano[3,4,b]indol]-4-amine for treating fibromyalgia and chronic fatigue syndrome The invention relates to a pharmaceutical dosage form comprising (1r,4r)-6'-Fluoro-(N- methyl- or N,N-dimethyl-)-4-phenyl-4',9'-dihydro-3'H-spiro-[cyclohexane-1,1'-pyrano[3,4,b]- indol]-4-amine or a physiologically acceptable salt thereof, for use in the treatment of fibromyalgia or chronic fatigue syndrome.
US7514445 Heteroaryl amines as glycogen synthase kinase 3β inhibitors (GSK3 inhibitors) This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7—C(═NH)R21; R4 is an optionally substituted heterocycle provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.
CN102861005A Application of Eryngiolide A in medicine for promoting small intestine peristalsis The invention relates to application of Eryngiolide A in preparing a medicine for promoting small intestine peristalsis. The invention provides application of Eryngiolide A in preparing the medicine for promoting small intestine peristalsis. Pharmacological tests prove that Eryngiolide A has favorable function of promoting small intestine peristalsis. The application of Eryngiolide A in preparing the medicine for promoting small intestine peristalsis, which is provided by the invention, is disclosed for the first time. The skeleton type belongs to brand-new skeleton type, and the small intestine peristalsis promoting activity of Eryngiolide A is extremely strong, so that no possibility for providing any prompt by other compounds exists. Eryngiolide A has outstanding actual characteristics. Meanwhile, Eryngiolide A has outstanding progress in preparing the medicine for promoting small intestine peristalsis.
CN101336724A Health food for resisting oxidation The invention discloses a health food for oxidation resistance, composed of the active ingredients by weight as follows: 0.01-15% of nutrient selenium, 15-70% of taurine, 10-60% of nutrient zinc and 5-70% of L-arginine, in which selenium has the lipid peroxidation resistance, taurine effectively eliminates free radicals, zinc improves the activity of the body enzymes and L-arginine promotes to generate NO. The health food is produced by mixing the active ingredients with an amount of weight proportion according to the function thereof respectively, which can give full play to the role of alleviating fatigue. It is proven by the animal test that the health food has the function of alleviating fatigue.
EP1539715A1 Crystal forms of quinoxaline-2-carboxylic acid 4-carbamoyl- 1-(3-fluorobenzyl)-2,7-dihydroxy-7-methyl-octyl -amide The invention relates to crystal forms of quinoxaline-2-carboxylic acid [4-carbamoyl-1-(3-fluorobenzyl)-2,7-dihydroxy-7-methyl-octyl]-amide, useful in treating or preventing a disorder or condition by antogonizing the CCR1 receptor, and to their methods of preparation and use.
WO2014063631A1 Tyrosine kinase irreversible inhibitor and preparation method and applications thereof The present invention provides a tyrosine kinase irreversible inhibitor shown in formula I or a pharmaceutically acceptable salt thereof, a preparation method for the tyrosine kinase irreversible inhibitor and applications of the tyrosine kinase irreversible inhibitor. The present invention belongs to the field of pharmaceutical chemistry. The tyrosine kinase irreversible inhibitor or the pharmaceutically acceptable salt thereof is very high in activity of inhibiting growth of cancer cells, and is especially remarkable in effect of inhibiting the growth of cancer cells with high expression of EGFR and HER2.
US7132238 Method of determining a chemotherapeutic regimen based on ERCC1 expression The present invention relates to prognostic methods which are useful in medicine, particularly cancer chemotherapy. The object of the invention to provide a method for assessing ERCC1 expression levels in fixed or fixed and paraffin embedded tissues and determine a platinum-based chemotherapy by examination of the amount of ERCC1 mRNA in a patient's tumor cells and comparing it to a predetermined threshold expression level. More specifically, the invention provides to oligonucleotide primer pair ERCC1 and methods comprising their use for detecting levels of ERCC1 mRNA.
CN101112387A Smectite turbid liquor for treating non-infectious diarrhea and method for preparing the same The present invention discloses a montmorillonite suspension to treat non-infectious diarrhea, which is made by montmorillonite, glucose, sodium saccharin, vanillin, sodium benzoate and purified water with certain mix ratio by weight. The preparation method is that the montmorillonite is placed in a preparation tank, the water is added for soaking; then the excipients which are glucose, sodium saccharin, vanillin, sodium benzoate are added and the purified water is supplemented to the prescription dose, fully agitated, the liquid is placed in a colloid mill for milling and refining, after that the liquid can pass through a 325 mesh screen, the screened liquid is cooled down to room temperature after the agitating under the heating condition, the purified water is supplemented to the prescription dose, then the invention is made by fully agitating. Montmorillonite is made into the suspension, thus having finer particles, greater absorption force, stronger effects of gastrointestinal mucosal protection and elimination of pathogens, and faster application of the pharmacological role.
US20120316176 DERIVATIVES OF 7,8-DIHYDRO-1H-IMIDAZO[2,1-b] PURIN-4(5H)-ONE and METHODS OF USE THEREOF The present invention relates to derivatives of 7,8-dihydro-1H-imidazo[2,1-b]purin-4(5H)-one, compositions thereof and methods of use thereof for treating or preventing pain or an inflammatory disease.
US20080213345 Delivering Iron to an Animal The invention provides a method for delivery iron to an animal. This invention further provides a method for treating iron deficiency in an animal.
CN102917687A Injectable emulsion of sedative hypnotic agent The present invention provides novel pharmaceutical formulations of a substituted phenylacetic acid ester compound, which is useful as a short-acting sedative hypnotic agent for anesthesia and sedation. The pharmaceutical formulations are oil-in-water emulsions suitable for administration by injection. The invention further provides processes for the preparation of the formulation and the use of the formulation in medical treatment of a mammal.
CN1995068A Angelica polysaccharide iron and its preparing process The invention discloses a chiretta ferric polysaccharide, which comprises the following steps: adopting high-quantivalent ferric compound blood tonic to provide raw material; extracting anoelica sinensis polysaccharide from anoelica sinensis through boiling in the water; dripping iron trichloride solution in the anoelica sinensis polysaccharide solution; displaying the adsorbing peak and corresponding chemical group irradiated by infrared spectrum: -OH and -NH extension vibration near 3400cm-1, -C-H extension vibration near 2930cm-1, -C-O vibration of amide carbonyl near 1620cm-1, -C-O vibration of carboxyl near 1400cm-1, C-O-H and C-O-C vibration near 1050 cm-1, adsorbing peak at 855cm-1 and 680cm-1.
WO2008088810A2 Formulations for cosmetic and wound care treatments with photosensitizers as fluorescent markers Photoactive materials, such as photosensitizers, are used as fluorescent markers for in vivo detection of the distribution of the injected filler material during cosmetic treatments. In one preferred embodiment, liposomal formulated temoporfin is used, as the photoactive component, in very small concentrations along with fillers for cosmetic and wound healing applications. Fillers, which can be used in the invention, include collagen, hyaluronic acids and other synthetic or natural products which are generally used in wound healing, scar reduction and other such medical applications. In a preferred embodiment, the formulated photosensitizer is coupled to the filler so that tracking is possible over longer periods of time A liposomal formulated photosensitizer is injected with the fillers into the treatment area, and is irradiated with laser light shortly after injection. The emitted fluorescence is measured by a special non-invasive device. Thereby it is possible to monitor the injection site and the distribution of the injected solution around the injection site. When irradiated with laser or other light source, the fluorescence of the photosensitizer is detected using a fluorescence detector, which permits tracking the filler at injection site and in the injection volume.
CN101790513A 1,3-dihydroisoindole derivatives The invention relates to novel 1,3-dihydroisoindole derivatives of formula (I), in which R1 - R3 are defined as cited in claim 1. Said derivatives are HSP90 inhibitors and can be used to produce a medicament for treating diseases, in which the inhibition, regulation and/or modulation of HSP90 plays a part.
WO2014078895A1 Omega-3 analogues The present invention relates to new fatty acid analogues and to their use in cancer therapy, including antimetastatic therapy.
WO2011011330A3 Inhibitors of d-amino acid oxidase The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.
WO2006107936A1 The use of ezetimibe in the prevention and treatment of cholesterol gallstones This invention discloses the use of compounds of the azetidinone family in the prevention or treatment of cholesterol gallstone disease of the biliary tree in mammals. This invention is in the general area of cholesterol stones disease in the biliary tree and gallbladder. In particular, the invention evidences that the use of drugs that specifically block cholesterol intestinal absorption inhibit the onset of cholesterol stone disease in the biliary tree. These drugs act by decreasing biliary cholesterol secretion, and at the same time increasing the biliary flow and the hepatic secretion of endogenous compounds (e.g. bile salts, phospholipids) into the bile, hi turn, these endogenous compounds contribute to inhibiting cholesterol precipitation and the formation of gallstones in the biliary tree.
WO2011055561A1 Protein crosslinking inhibitor and use thereof Disclosed are: a ketone compound which is represented by general formula (1), (2) or (3) and has transglutaminase inhibitory activity; a protein crosslinking inhibitor which contains the compound; and a composition for prevention or treatment of diseases that are caused by crosslinking of proteins, said composition containing the compound or the protein crosslinking inhibitor. (In the formulae, R1 represents a substituted or unsubstituted aryl group or heterocyclic group; R2, R3 and R4 each represents a hydrogen atom; n represents 2; X represents a halogen atom; and R5 and R6 each independently represents a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl group, aryl group or aralkyl group. In this connection, R5 and R6 are not hydrogen atoms at the same time, and R5 and R6 may combine together to form a saturated or unsaturated, substituted or unsubstituted heterocyclic group that contains a nitrogen atom (N).)
CN102764429A Composition used for increasing regulatory T cells in vivo and use thereof The present invention discloses a composition used for increasing regulatory T cells in vivo and the use thereof. The composition used for increasing regulatory T cells in vivo is characterized in that the composition contains 20-50*10<4> I. U. of interleukin-2 and 0.05-10.5 mg of glucocorticoid.
CN101066465A Antitumor use of antisense thionucleotide The present invention relates to one kind of medicine composition including antisense thionucleotide 5'-CTC CCA GCG TGC GCC ATC-3' in the clinical dosage of 5-20 mg/kg and pharmaceutically acceptable carrier. In extracorporeal cultured human lung cancer cell line, the antisense thionucleotide with Bcl-2 protein mRNA as target point can inhibit the expression of the cancer causing gene bcl-2 effectively and specifically and make the cancer cell die in obvious early apoptosis effect. The animal model test shows that the antisense thionucleotide can inhibit the growth of tumor in human lung cancer induced nude mice obviously, with the inhibition rate in 20 mg/kg dosage reaching 90 %. The antisense thionucleotide and its medicine composition are suitable for use in preparing antitumor medicine.
US7048928 Inhibitor of histamine synthesis, especially of of histidine decarboxylase such as tritoqualine; allergen, e.g., cysteine protease The present invention relates to an anti-allergic pharmaceutical composition containing at least two active agents chosen from among: (i) one allergen, (ii) one antihistamine compound, and (iii) one inhibitor of histamine synthesis. The active agents are associated in the composition with a pharmaceutically acceptable vehicle.
EP2763994A2 Novel quinoxaline inhibitors of pi3k The invention provides methods that relate to a novel therapeutic strategy for the treatment of cancer and inflammatory diseases. In particular, the method comprises administration of a compound of Formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such compound admixed with at least one pharmaceutically acceptable excipient.
US20100209400 TAK1-Mediated Regulation of Osteogenesis This invention is directed to methods, nucleic acids and compositions in TAK1-mediated regulation of SMAD activity. Promotion of TAK1 interaction with MH2 domains in SMADs negatively regulates SMAD biological activity. BMP-mediated SMAD activity is subject to TAK1 effects.
CN103705528A Compound colinflosaxin soluble powder for preventing and treating poultry colibacillosis The invention discloses compound colinflosaxin soluble powder for preventing and treating poultry colibacillosis. The soluble powder is prepared from the following components in percentage by weight: 4-10 percent of colinflosaxin, 5-10 percent of florfenicol sodium succinate, 3-10 percent of neomycin sulfate, 3-8 percent of trimethoprim lactate and the balance of pharmaceutically acceptable auxiliary materials. The drug resistance of escherichia coli is seriously considered, every pathogenic microorganism is considered, the reasons of harming the organisms are comprehensively considered, the antibacterial spectrum is wide, and the soluble powder is effective to multiple escherichia coli strains and is high in antimicrobial activity. Moreover, novel antibacterial agents such as colinflosaxin and florfenicol sodium succinate are adopted and are combined; compared with that of a conventional antibacterial agent, the antibacterial property of the soluble powder is greatly improved, and secondary infection can be effectively controlled.
CN1785161A Magnetic nano-balls carried with cisplatin and its prepn. method A magnetic nanoball carrying cisplatin is disclosed, which can be used as the medicine carrier to provide magnetic targetability. Its preparing process includes such steps as preparing the carboxypolyose modified Fe3O4 nanopartieles by chemical codeposition method under existence of carboxypolyose, and coordination between the free carboxy in carboxypolyose on the surface of Fe3O4 nanoparticle and Pt atoms for coupling the cisplatin with said nanoparticle. It can be used for the controlled slow-release medicine applying system.
CN102993212A Picrinine salt and pharmaceutical application thereof The invention relates to a picrinine salt or a pharmaceutically acceptable solvate thereof, and a pharmaceutical application thereof in preparing medicines used for treating and/or relieving coughing.
CN102125525A Orally disintegrating tablet with rivastigmine tartrate The invention discloses an orally disintegrating tablet with rivastigmine tartrate. The orally disintegrating tablet comprises a main drug of rivastigmine tartrate and supplementary materials of microcrystalline cellulose, mannitol, lactose, crosslinked polyvinylpyrrolidone, sodium cyclamate, menthol, silica gel micropowder and magnesium stearate. The orally disintegrating tablet with the rivastigmine tartrate can be used for effectively treating Alzheimer's disease, is conveniently taken and quickly disintegrated, has a favorable mouth feel and high bioavailability and provides convenience for Alzheimer's disease patients who take medicine inconveniently.
WO2009152712A1 Vinflunine salts, preparation process and pharmaceutical composition thereof The present invention provides vinflunine salts of formula (I), a process for preparing them and their pharmaceutical composition. M and n in the formula (I) are defined as in the specification.
CN102160859A Loratadine and pseudoephedrine compound slow-release medicament The invention discloses a loratadine and pseudoephedrine compound slow-release medicament. The loratadine and pseudoephedrine compound slow-release capsule provided by the invention is formed by mixing a pill A and a pill B, wherein the pill A comprises pseudoephedrine sulfate, loratadine, carboxymethylcellulose sodium, microcrystalline cellulose, hydroxypropyl methylcellulose, ethyl cellulose and talcum powder; and the pill B comprises pseudoephedrine sulfate, loratadine, carboxymethylcellulose sodium, microcrystalline cellulose, hydroxypropyl methylcellulose and talcum powder; The loratadine and pseudoephedrine compound slow-release capsule (I) prepared by the invention can obviously and continuously control common symptoms of common cold or influenza, and has better treatment effect and tolerance. The slow-release capsule is slightly influenced by gastrointestinal food evacuation after being orally taken, thus the individual difference of medicament absorption is small. Moreover, the area of the medicament distributed on the surface of the gastrointestinal tract is increased, thus the gastrointestinal adverse reaction caused by local stimulation of the medicament can be reduced.
US8546344 Crystalline phases of 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl)-1H-benzimidazole The invention relates to novel crystalline phases of 5,6-dichloro-2-(isopropylamino)-1-(β-L-ribofuranosyl)-1H-benzimidazole (Maribavir), pharmaceutical compositions thereof and their use in medical therapy.
US6984629 Such as uridine 5'-diphosphoric acid for corneal epithelial migration promotion Based on research for compounds that can display a corneal epithelial migration promoting effect in ophthalmology, the present invention provides P2Y receptor agonist corneal epithelial migration promoters, such as phosphoric acid compounds having an adenosyl group, uridyl group, xanthosyl group, guanosyl group, or thymidyl group, or their salts, with excellent corneal epithelial migration promoting effects.
WO2006098342A1 Piperazinyl compounds A compound of formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar is aryl or heteroaryl, optionally substituted; R1 is acyl; R2 is H or lower alkyl; R3 is H, and the like; R4 is H, and the like.] having the activity inhibiting DPP-IV activity. They are therefore useful in the treatment or prevention of conditions mediated by DPP-IV, such as Type 2 Diabete Mellitus.
US8465767 Mixture with tablet distegrant; sustained release; embedding water soluble particle in plastic membrane coating ; stomach disorders The invention relates to an oral administration form for pyridin-2-ylmethylsulfinyl-1H-benzimidazoles and their salts, which comprises the active compound together with tablet disintegrants and is provided with a film coating customary per se for sustained-release compositions.
CN103083253A Lyophilized preparation of acetaminophen and preparation method thereof The present invention relates to a lyophilized preparation of acetaminophen. The lyophilized preparation is obtained by lyophilization, including: 0.5-5% of acetaminophen, 0.5-30% of a lyophilization protectant, 0.01-5% of a chelant, 0.01-5% of a pH adjusting agent, 0.01-5% of an antioxidant and the balance being a solvent. The lyophilized preparation of acetaminophen and a preparation method thereof provided by the invention help to overcome that the lyophilized preparation is vulnerable to moisture, oxygen, pH, temperature, light and other factors in the prior art. The invention provides the lyophilized preparation of acetaminophen which is good in stability and high in safety performance.
US20080051341 Medicament for treatment of non-insulin dependent diabetes mellitus, hypertension and/or metabolic syndrome A substance including the chemical structures of bicyclo[3.2.1]octan or the chemical structures of kaurene for the use in a dietary supplementation or as a constituent in a medicament for the treatment of non-insulin dependent diabetes mellitus, hypertension and/or the metabolic syndrome. The unique chemical structures of bicyclo[3.2.1]octan alone or in a kaurene structure provides the substances, such as e.g. steviol, isosteviol and stevioside with the capability of enhancing or potentiating the secretion of insulin in a plasma glucose dependent manner. The substances including these unique chemical structures also have the capability of reducing the glucagon concentration in the blood and/or lowering the blood pressure thereby providing a self-regulatory treatment system for non-insulin dependent diabetes mellitus and/or hypertension. In a combination drug which also comprise a soy protein, and/or soy fiber and/or at least one isoflavone these substances act synergistically and such combination drugs are highly useful both prophylacticly or directly in the treatment of e.g. the metabolic syndrome and obesity and has due to the self-regulatory effect a widespread applicability as a dietary supplementation.
US20110200580 Methods of treatment and prevention of diet-induced obesity and sequelae thereof Disclosed are methods of treating or preventing diet-induced obesity and/or one or more sequelae thereof in a subject. These methods comprise administering to a subject in need of treatment or at risk for developing diet-induced obesity and/or one or more sequelae thereof, a therapeutically effective amount of a pharmaceutical composition comprising at least one inhibitor of RP 105 and/or MD-I activity. Also disclosed are methods of identifying compounds that inhibit development of diet-induced obesity and/or one or more sequelae thereof. In some aspects, these methods comprise: providing at least one first cell comprising TLR4, MD-2. RP105. MD-K and a TLR4-responsive promoter operably linked to a nucleic acid sequence encoding a reporter, contacting the at least one first cell with lipopolysaccharide and with a candidate compound; and determining a level of expression of the reporter in the presence of the LPS and the candidate compound, in some aspects, these methods comprise: providing at least one first cell comprising TLR2, TLR1, TLR6, MD-2, RP H/S, MD-K and a TLR2-responsive promoter operably linked to a nucleic acid sequence encoding a reporter, contacting the at least one first cell with a lipopeptide ligand of TLR2 and with a candidate compound, and determining a level of expression of the reporter in the presence of the lipopeptide ligand of TLR2 and the candidate compound
CN101624332B New compound with anti-tumor activity and application thereof The invention provided a compound with the formula (I), pharmaceutically acceptable salt or stereoisomer and the application thereof, and the group definition is explained in specification. The provided new compound has the functions of inhibiting tumour cell proliferation and blocking the generation of tumour blood vessels, thus providing a new antineoplastic in clinical practice.
CN102885832A Application of Gypensapogenin A in medicine for treating rhinitis The invention discloses Gypensapogenin A for treating immune inflammation. The Gypensapogenin A is used for preparing a medicine for treating the immune inflammation, is especially suitable for preparing a medicine for treating rhinitis, and is definite in curative effect by using terfenadine and diclofenac sodium as contrasts. The application of Gypensapogenin A in preparation for the medicine for treating the immune inflammation is initially disclosed; Gypensapogenin A has prominent substantive features due to a brand new framework type, an unexpected treatment activity for rhinitis and no possibility of giving any revelation by other compounds; and simultaneously, Gypensapogenin A obviously has a remarkable progress in case of being used for prevention and treatment for rhinitis.
CN102028951B RGDfK-modified oridonin polylactic acid medicament-carrying nanoparticles and preparation method thereof The invention discloses a preparation method of RGDfK-modified oridonin polylactic acid medicament-carrying nanoparticles. In the method, based on the preparation of oridonin polylactic acid nanoparticles by an improved self-emulsification solvent diffusion method, composite polypeptide condensing agents, namely, EDC.HCl and NHS-sulfo are selected and a two-step condensation reaction is performedso as to prepare ORI-NP-RGDfK. The ORI-NP-RGDfK prepared by the method has the characteristics of remarkable sustained release, good selective distribution for tumors, good anti-tumor effect on mice transplanted liver cancer, remarkable tumor necrosis, remarkably prolonged life cycle, improved life quality and remarkable anti-tumor effect superior to those of an ORI group and an ORI-NP group (P is smaller than 0.05).
WO2009157505A1 Telomerase inhibitor Disclosed is a compound having strong telomerase inhibitory activity. The compound has a macrocyclic structure, which is represented by general formula (1) and composed of seven oxazoles, and a side chain containing an amino group. (In the formula, X represents -CH2-, -NHC(NH)-, -CH(NH2)-, -C(NH)-, -NHCO-, -CO-, -NHCONHC(NH)-, a cyclohexadienylene group, or a 3,4,5,6-tetrahydropyrimidin-2,6-yl group; R1 represents a single bond, an alkylene group having 1-12 carbon atoms, an alkenylene group having 1-12 carbon atoms or an alkynylene group having 1-12 carbon atoms; and R2-R7 independently represent a hydrogen atom or the like.)
WO2009101956A1 Novel substance fki-3864 and method for production thereof Disclosed is a substance FKI-3864 which is represented by formula [I] and has an inhibitory activity on the production of triacylglycerol. Also disclosed is a method for producing the substance FKI-3864. The method for producing the substance FKI-3864 comprises the steps of: culturing a microorganism belonging to the genus Penicillium and capable of producing the substance FKI-3864, particularly Penicillium pinophilum FKI-3864 (FERM P-21483) to accumulate the substance FKI-3864 in a culture; and collecting the substance FKI-3864 from the culture. The substance has an inhibitory activity on the production of triacylglycerol in a cell, and is useful for the prevention or treatment of obesity.
US20120309788 Method for Treating Alzheimer's Disease Using Pharmacological Chaperones To Increase The Activity of Gangliosidases The present invention relates to a method for treating an individual having Alzheimer's Disease by using pharmacological chaperones to increase the activity of gangliosidase and/or sialidase enzymes involved in ganglioside catabolism.
EP1594494A1 Oxazolidinone derivatives n-substituted by a bicyclic ring, for use as antibacterial agents Compounds of formula (I) and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula (I) as well as pharmaceutically acceptable compositions comprising compounds of formula (I). Compounds of formula (I) as disclosed herein can be used in a variety of applications including use as antibacterial agents. P is a bicyclic ring system as defined in claim 1.
WO2012172090A1 Chromane-like cyclic prenylflavonoids for the medical intervention in neurological disorders The present invention relates to certain chromane-like cyclic prenylfiavonoids, in particular the compounds of formulae (I), (II) and (III) as described and defined herein, for use in the treatment or prevention of a neurological disorder, as well as their use in promoting neuronal differentiation, neurite outgrowth and neuroprotection.
US20120064027 Absorbable adhesive paste An absorbable adhesive paste contains absorbable solid carboxy-bearing microparticles dispersed in a continuous phase of an alkoxyalkyl cyanoacrylate. The paste may contain a soluble absorbable polymeric viscosity modifier and at least one bioactive agent to maximize the effective application as a cover for compromised tissues and wounds or as sealants, blocking agents, or hemostatic agents.
CN103127128A Cefpirome sulfate pharmaceutical composition powder injection The invention provides a cefpirome sulfate pharmaceutical composition powder injection, relating to the field of a pharmaceutical preparation and a preparation method thereof. The invention solves the problems of high dosage of single cefpirome sulfate and metronidazole preparation, poor treatment effect after combination, and great side effect at present. The main materials of the pharmaceutical composition are cefpirome sulfate and metronidazole lipid microspheres, the auxiliary material is sodium carbonate, the weight ratio of the cefpirome sulfate (on the basis of cefpirome) to the metronidazole lipid microspheres (on the basis of metronidazole) is 100:6-100:20, and the weight ratio of the cefpirome sulfate (on the basis of cefpirome) to the sodium carbonate is 1000:242; and after the pharmaceutical composition is prepared into the powder injection, the pH value of the water solution of the pharmaceutical composition is 5.5-7.0. The pharmaceutical composition powder injection provided by the invention has high curative effect, and can reduce the consumption of the metronidazole by more than 80%, thereby greatly relieving or avoiding the toxic and side effects of the metronidazole, especially digestive tract reactions, including nausea, vomit, inappetence, abdominal colic and neurotoxicity, and lowering the incidence rate of adverse reactions.
WO2008130581A1 Pyrimidinone derivatives and methods of use thereof The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of G protein-coupled receptor 119 ('GPR119') in a patient.
CN103432095A Intra-gastric floating sustained-release preparation of cefalexin and preparation method thereof The invention relates to an intra-gastric floating sustained-release preparation of cefalexin which can be taken once every day and a preparation method thereof. The preparation comprises the following components in percentage by weight: 65-85wt% of cefalexin as active constituent, 5-15wt% of water-swelling polymer, 4-14wt% of hydrophobic material of which the density is small than gastric juice and 3-7wt% of a foaming agent. The preparation can release cefalexin in a stable and sustained releasing manner in 6-24 hours.
CN103736083A Composition for detoxifying, beautifying and slimming The invention provides a composition for detoxifying, beautifying and slimming, which is prepared from ginseng, wolfberry, platycodon root, lily, lotus seeds, peach kernel, donkey-hide gelatin, hawthorn, senna leaf, grape seed, cordyceps and other herbal medicines. The composition provided by the invention has the definite effects of detoxifying, beautifying and slimming.
US20080051363 G-rich polynucleotides as a novel therapeutic for the treatment of huntington's disease The present invention relates to oligonucleotide compositions and therapeutic uses thereof to modify protein-protein interactions. In particular, the invention relates to the use of a guanidine-rich oligonucleotides to disrupt disease-causing protein aggregates, for example, Huntington's Disease (HD) protein aggregates
US20090162406 Wound healing with zeolite-based hemostatic devices A method for decreasing the time it takes for a wound to heal includes applying hemostatic agent to the wound, inflaming tissue surrounding the wound to facilitate the deposition of fibroblast, thereby accelerating the subsequent contraction of the wound and the onset of the proliferative healing stage, and causing the re-epithelization of the tissue at a faster rate than if no hemostatic agent was applied. A method for promoting the healing of a bleeding wound includes coating a hemostatic agent onto a substrate, applying the substrate to the bleeding wound so that an effective amount of the hemostatic agent is applied to the wound, inflaming the tissue, and causing the re-epithelization of the tissue at a faster rate than if no hemostatic agent was applied. In at least some methods, a clotting cascade and platelet aggregation within the bleeding wound is accelerated, and blood loss from the wound is decreased.
US7115615 Antitumour agents as enzyme inhibitors of the nonreceptor tyrosine protein kinases involved in the signal transduction; noninvasive; antimetatic and -carcinogenic agents; derivatives of 4-(1,3-benzo-dioxol-4-yl)amino-)quinazoline The invention concerns quinazoline derivatives of Formula (I) wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
CN1836666A Water-soluble vitamin for injection and its preparation process and quality control method The present invention discloses water soluble vitamins for injection and its preparation process and quality control method. Of the high quality water soluble vitamins for injection, each unit container contains thiamine nitrate 2.8-3.4 mg, nicotinic amide 36-44 mg, vitamin B6 hydrochloride 4.4-5.4 mg, sodium pantothenate 14.8-18.1 mg, sodium cytoflavin 4.4-5.4 mg, vitamin C sodium 102-124 mg, biotin 54-66 mcg, folic acid 0.36-0.44 mg, vitamin B 12 4.5-6.0 mcg and methyl solbrol 0.4-0.6 mg. The water soluble vitamins for injection has high controllability, high stability and long preservation period.
US7390502 Administering a mammalian host for treating a disease caused by proliferation of eukaryotic cells a formulation containing a complex of lipid and a drug 7-ethyl-10-hydroxycamptothecin The present invention is for novel compositions and methods for treating diseases caused by cellular proliferation, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include SN-38 lipid complexes in which the complexes can contain any of a variety of neutral or charged lipids and, desirably, cardiolipin. The compositions are capable of efficiently incorporating SN-38 into complexes and are capable of solubilizing relatively high concentrations of SN-38.
CN1875951A Soft capsule of sodium houttuyfonate and preparation method thereof The invention relates to a soft capsule containing effective composition of sodium houttuyfonate and process of preparation, wherein the capsule is prepared mainly from sodium houttuyfonate as the main ingredient, and has the advantages of high dissolving rate, quick effect, high biological availability, convenience in administration and carrying.
WO2010117992A2 Coupled identification and treatment of cancer Provided are methods to treat cancer in which a patient is identified as having gallium-avid cancer by use of a gallium scan or other means, and is then treated with a pharmaceutically acceptable gallium composition.
US20130005698 Pharmaceutical for preventing or treating an inner ear disorder A pharmaceutical for preventing or treating an inner ear disorder, comprising a spirohydantoin derivative represented by a general formula (I): in the formula, X represents a halogen atom or a hydrogen atom, and R1 and R2 simultaneously or individually represent a hydrogen atom or an optionally substituted C1-6 alkyl group, or a pharmacologically acceptable salt thereof as an active ingredient.
WO2008104278A1 Imidazo[1,2-a] pyridines and their use as pharmaceuticals The present invention relates to derivatives of imidazo[1,2-a]pyridines of the formula (I), in which R, R1 to R4 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula (I) upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula (I), to pharmaceutical compositions comprising them, and to the use of compounds of the formula (I) for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
US20110105567 Pyrrole Compounds Having Sphingosine-1-Phosphate Receptor Agonist Or Antagonist Biological Activity Disclosed herein are compounds represented by: therapeutic methods, compositions, and medicaments related thereto are also disclosed.
US20120208783 Medicine, Food And Drink Or Feed Containing Sphingomyelin It is intended to find novel pharmaceutical use of sphingomyelin and to provide preventive or therapeutic agents for various diseases as well as a food and drink product and feed comprising any of these agents. The present invention provides a pharmaceutical agent which contains sphingomyelin as an active ingredient and is any of the following agents: 1) a sialomucin secretion promoter, 2) an agent for preventing drunken sickness (hangover), 3) an antiallergic agent, 4) an antioxidant, 5) an agent for defending against infection, 6) a hair growth agent, 7) a therapeutic agent for demyelinating disease, 8) an anti-pigmentation agent, 9) an anti-inflammatory agent, and 10) an agent for improving learning ability. The present invention also provides a food and drink product or feed, characterized by comprising the agent. It is preferred that the sphingomyelin should be derived from milk.
WO2010006191A1 4-phenoxymethylpiperidines as modulators of gpr119 activity The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.
EP1575970A2 10-substituted macrolide antibiotics The application provides antibiotic 10-substituted 10-desmethyl macrolides. In a preferred embodiment the macrolides have an erythromycin basic structure according the formula, wherein the variable substituents have the meaning indicated in the description.
US7786172 percutaneously; cyclical mastalgia; may be formulated in a hydroalcoholic gel or an alcoholic solution A method of treatment comprises administering 4-hydroxy tamoxifen percutaneously to a patient having mastalgia. The 4-hydroxy tamoxifen may be formulated in a hydroalcoholic gel or an alcoholic solution.
US20110158982 COMPOSITIONS AND METHODS FOR INHIBITING MAdCAM The present invention relates to therapeutic targets for multiple sclerosis and neuroinflammatory diseases and injuries. In particular, the present invention relates to targeting MAdCAM in the treatment of such disorders.
US20080227705 Apoptosis-inducing agent and method for inducing apoptosis An object of the present invention is to provide a novel means for stably and surely inducing cell apoptosis using the c-myc gene as a target. The present invention relates to an apoptosis-inducing agent containing a protein that interacts with an FBP protein or a polynucleotide encoding the protein as an active ingredient and a method for inducing apoptosis, which comprises a step of causing the apoptosis-inducing agent to come into contact with cells.
US8518447 Method for treating or preventing renal or liver disease The methods for treatment using an adsorbent having a high adsorbability, and capable of adsorbing a large amount of toxins during a retention period in an intestine, and of remarkably increasing an adsorption amount of compounds having a large molecular weight.
CN103251667A Application of general inula helenium sesquiterpene lactone in preparation of medicine for treating rheumatoid arthritis The invention provides application of general inula helenium sesquiterpene lactone in preparation of a medicine for treating rheumatoid arthritis. The general inula helenium sesquiterpene lactone contains alantolactone and isoalantolactone; and the sum of the contents of the alantolactone and the isoalantolactone accounts for 60 to 90%. The results of animal pharmacodynamic tests show that the general inula helenium sesquiterpene lactone, the alantolactone and the isoalantolactone all can inhibit the clinical onset of CIA (Collagen-induced Arthritis), obviously inhibit the morbidity of CIA, obviously reduce the level of IFN(Interferon)-gamma, and remarkably inhibit the generation of IL(Interleukin)-17. Therefore, the general inula helenium sesquiterpene lactone, the alantolactone and the isoalantolactone all can be used for preparing the medicine for treating rheumatoid arthritis. The medicine is composed of the general inula helenium sesquiterpene lactone serving as an active ingredient and a pharmaceutic adjuvant and can be in form of a troche, a capsule, a soft capsule, a dropping pill, granules, an injection, a powder-injection or an aerosol and the like. The medicine provided by the invention is a new medicine for treating rheumatoid arthritis, which has remarkable curative effect and little side reaction; the raw materials are conveniently obtained, the preparation method is simple, and the medicine has relatively high clinical application value.
WO2008092396A1 Microcapsule formulation of kitasamycin, process for preparation thereof and use thereof A microcapsule formulation of kitasamycin, a process for the preparation thereof, and the use thereof in the manufacture of an antibacterial growth promoting agent for fowl and livestock, wherein the microcapsule formulation contains kitasamycin and a pharmaceutical excipient, the weight of said pharmaceutical excipient is 2 - 16 times of kitasamycin, the pharmaceutical excipient is selected from one or more of glyceryl monostearate, fat powder, C12-18 fatty acid such as stearic acid. The said microcapsule formulation is prepared by: melting the pharmaceutical excipient by heating, blending it with kitasamycin until homogeneous, then spray-cooling.
WO2007116228A1 Piperidine derivatives for treatment of alzheimer's disease Compounds of formula (I) modulate the activity of gamma secretase and hence find use in treatment or prevention of Alzheimer's disease and related conditions.
CN1927278A Children's Shuangqing dispersant tablet and method for making same The invention relates to dispersible tablets for treating fever in children and method for preparation, wherein the raw materials of the medicament include artificial ox gallstone, antelope's horn, buffalo horn concentrated powder, magnolia bark, isatic root, capsule of weeping forsythia, bistort, gypsum, radish seeds, schizonepeta spike, menthol, boneol.
CN1660058A Application of zinc taurine in preparing medication for anti anoxia An application of zinc taurinate in preparing the medicines for treating anoxic diseases is disclosed.
CA2605298A1 Crystal of hydroxynorephedrin derivative hydrochloride 1/4 hydrate There is provided ethyl (-)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride 1/4 hydrate or its crystal, which can be identified by characteristic diffraction peaks of powder X-ray diffractometry, differential scanning calorimetry, etc., obtained by producing, through specified process, ethyl 2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate.
US7763652 such as 9-Deoxy-9 beta -chloro-16,17,18,19,20-pentanor-15-cyclohexyl-2,2,3,3,13,14-hexadehydro-6-thia-prostaglandin F1, useful as drugs for sleep induction A prostaglandin derivative represented by Formula (I): wherein X is a halogen atom in the α- or β-substitution, Y is an ethylene group, a vinylene group or an ethynylene group, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with a C1-4 straight or branched chain alkyl group or a C4-13 cycloalkylalkyl group, R2 is a hydrogen atom or a CO2R3 group (R3 is a hydrogen atom, a C1-4 straight or branched chain alkyl group or a C2-4 straight or branched chain alkenyl group), n is an integer of 1 to 4 and p is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.
US20120058193 Injectable smart gel and method for fabricating the same An injectable smart gel and a method for fabricating the same are disclosed. A basic structural stabilizer/polymeric electrolyte and a diluting solution are added to a modified chitosan to regulate the chitosan solution to have a pH value closing to that of the human body and form a flowable chitosan sol. The flowable chitosan sols formed thereby are respectively converted into inflowable chitosan gels via increasing the temperature thereof to the human body temperature, and via adding calcium ion or regulating the chitosan sol into an acidic solution. The injectable smart gel fabricated thereby is injectable and able to function as a carrier of magnetism-sensitive medicine-containing nanocapsules. The medicine can be released to the injectable smart gel with an external non-contact force, such as a magnetic field, an electric field or an ultrasonic wave, for long-acting and multi-stage medicine delivery. The present invention is very useful in biomedical engineering.
CN1846786A Vaccins vivants recombines et adjuves The invention concerns a recombinant live vaccine comprising a viral vector incorporating and expressing in vivo a heterologous nucleotide sequence, preferably a pathogenic agent gene, and at least a adjuvant compound selected among the acrylic or methacrylic polymers and the maleic anhydride and alkenyl derivative copolymers. It concerns in particular an acrylic and methacrylic acid polymer cross-linked with a sugar or polyalcohol polyalkenyl ether (carbomer), in particular crosslinked with a saccharose allyl or with allylpentaerythritol. It can also be a maleic anhydride and crosslinked ethylene copolymer, for example divinylether. .
CN103588851A Novel hecogenin compound and extract and preparation method and application thereof The invention relates to a novel hecogenin compound with a structural formula (I): (novel hecogenin,3-O-beta-D-glucose-(1-2)-[beta-D-glucose-(1-3)]-beta-D-glucose-(1-4)-beta-D-galactoside); after the reflowing extraction of C.tuberosum harb ethanol, obtained crude extract is implemented with column chromatography by macroporous resin, and is gradually eluted by water and ethanol; the obtained 70% ethanol eluate is implemented with ODS column chromatography, and is eluted by water and 100% acetonitrile; the 70% ethanol eluate has the purpose of inducing platelet aggregation activity aspect.
CN102188428A Compound preparation of amlodipine and nicotinic acid The invention provides a compound preparation of amlodipine and nicotinic acid. The two active ingredients, namely the amlodipine and the nicotinic acid, are in the same independent preparation, wherein the nicotinic acid is in a medicament release unit with sustained-release effect. The medicament release unit with the sustained-release effect also comprises sustained-release carrier, adhesive, lubricant and other necessary pharmaceutically-acceptable excipients. The sustained-release carrier is selected from cellulose or derivative thereof with good expansibility and gelling property, namely hydroxy propyl cellulose, hydroxypropyl methylcellulose, methylcellulose, hydroxyethyl cellulose or mixture thereof. The compound preparation can better control multiple dangerous spectrums of coronary heart disease, atherosclerosis and stenocardia so as to prevent or reduce the coronary heart disease, the atherosclerosis and the stenocardia. The compound preparation can be used for treating mammalian hyperlipidemia with hypertension, and can also be used on mammals without heart risk to achieve heart disease risk control effect.
CN102727477A Application of retinoic acid and its derivatives in preparation of drugs preventing and treating diabetes The invention discloses application of a retinoic acid and its derivatives in preparation of drugs preventing and treating diabetes. The retinoic acid and its derivatives can inhibit the occurrence of inflammation induced insulin resistance by inhibiting AP-1 activity, thus further delaying and relieving the occurrence and symptoms of type II diabetes. Therefore, retinoic acid and its derivatives are a drug candidate molecule that boasts great development prospects and is used for prevention and treatment of type II diabetes. By giving the retinoic acid and its derivative compounds as well as preparations, diabetes attacks can be inhibited and blocked. At the same time, the small molecular drugs adopted in the invention are characterized by easy acquisition, low price, stable property, as well as convenient storage and transport.
CN101891768A 9-(diethoxy) phosphonomethyl purine, preparation method and application thereof in antineoplastic aspect The invention discloses an acyclic nucleoside phosphate compound, i.e. 9-(diethoxy) phosphonomethyl purine, a preparation method and application thereof in the antineoplastic aspect. The structural formula of the compound is shown as the following specification. In the preparation method, the 9-(diethoxy) phosphonomethyl purine is prepared by two reactions by using methylene diiodide, triethyl-phosphite and adenine as raw materials, using N,N-dimethyl formamide, dimethyl sulfoxide, methanol and ethanol as solvents and using anhydrous potassium carbonate and sodium methoxide as catalysts. The compound has a certain inhibiting effect on the hepatoma cell BEL-7402.
US20120148693 Herbal Drug Composition for Cartilage Protection The present invention relates to a herbal drug composition for cartilage protection comprising plant extracts of Clematis Radix, Trichosanthis Radix, and Prunellae Spica and an optimal content of rosmarinic acid to: (i) alleviate pains; (ii) inhibit the acute/chronic inflammation, platelet/whole blood aggregation, immunocyte (B-lymphcyte and T-lymphcyte) proliferation, inflammation-inducing enzyme activities, and enzyme activities associated with degradation of joint tissue; (iii) scavenge activity of toxic active oxygen radicals; and (iv) further provide excellent cartilage protection activity to be effectively used as an anti-inflammatory agent with analgesic effects, blood circulation enhancer, arthritis therapeutic agent and cartilage protective.
US7202246 Spiro-rifamycin derivatives targeting RNA polymerase Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the current invention relate to a series of novel spiro rifamycin derivatives which have demonstrated potent antimicrobial activity.
CN103520736A Floxuridine-layered double hydroxide nanohybrid with polyethylene glycol derivative modified on surface and preparation thereof The invention discloses a floxuridine(FL)-layered double hydroxide nanohybrid (LDH)surface-modified with polyethylene glycol monomethyl ether sebate(MPS), namely FL-LDH-MPS for short and a preparation method thereof, and aims to provide a method for preparing an MPS-modified FL-LDH nanohybrid by taking FL intercalated LDH (FL-LDH) nanohybrid as a model system and PEG derivative MPS with an invisible effect as a modifier. The nanohybrid is used for improving the dispersion stability and the invisibiity of the FL-LDH and improving the target delivery effect and the controlled release effect of FL so as to improve the pharmaceutical effect, reduce the toxic or side effect of the medicine and the like.
CN102178772A Mongolian medicament for strengthening muscles and bones, promoting blood circulation and removing blood stasis, diminishing inflammation and easing pain The invention discloses a Mongolian medicament for strengthening muscles and bones, promoting blood circulation and removing blood stasis, diminishing inflammation and easing pain, which is mainly prepared from the following raw materials in part by weight: 300 parts of Arula, 300 parts of Barula, 300 parts of Zhurula, 200 to 500 parts of phellodendron, 100 to 200 parts of clam, 200 to 500 parts of Zhugang, 100 to 300 parts of safflower and 100 to 200 parts of Ximuxing. The Mongolian medicament has the effects of strengthening muscles and bones, promoting blood circulation and removing blood stasis, diminishing inflammation and easing pain, removing dampness and dispelling wind and the like, is mainly used for treating traumatic injury, pain in necks, waists and backs, osteoproliferation, osteoarthritis, rheumatic arthritis, superficial thrombophlebitis, intervertebral disc herniation, ischioneuralgia, gout, femoral head necrosis and the like, and is suitable for various diseases and convenient to popularize and apply.
WO2011150566A1 Novel dna vaccine adjuvant The present invention discloses a novel DNA vaccine adjuvant, comprising a polysaccharide nucleic acid fraction from Bacillus Calmette-Guerin (BCG-PSN). BCG-PSN can augment the immunogenicity of DNA vaccine.
US20120015053 Treatment of psoriasis This invention relates to compositions, and methods of use thereof, for treating conditions associated with elevated arginase levels and/or activity comprising administering to a subject in need thereof, certain polyphenols such as flavanols, procyanidins, or pharmaceutically acceptable salts or derivatives thereof.
US20110311451 Synthesis of polymer conjugates of indolocarbazole compounds The present invention relates to a process for the preparation of polymer conjugates of iπdolocarbazole compounds, in particular of polymer conjugates of K-252a and derivatives thereof, by a synthetic route which results in a highly pure product, with a high product yield. In a further aspect the present invention relates to novel polymer conjugates of K-252a and derivatives thereof, wherein the chemical group linking the polymer unity to the K-252a or to the K-252a derivative compound is characterised by a 5-member oxazolidindionic cyclic structure. These novel polymer conjugates are obtained through the novel synthetic route with high purity and high yields,
CN101019954A Ecological vagina cleaning bacteriostasis liquid The present invention discloses one kind of ecological vagina cleaning bacteriostasis liquid, each 1000 ml of which contains lactobacillus polysaccharide 4-10 g, grape fruit extract 5-10g, lactic acid 10-15 ml, peppermint oil 0.5 ml, cocoanut amide propyl betaine 0.5ml; azone 2-5ml, ethanol solution (95 %) 200-250ml, and essence 1-2ml, except pure water. The present invention can reach the effects of cleaning surface and permeating to deep part to inhibit germ growth, regulate micro ecologic environment, and treat vulvitis, pudendal pruritus, etc.
CN103275141A Carbon 18 two double bonds diacetylation lactone sophorolipid and application thereof The invention discloses a compound carbon 18 two double bonds diacetylation lactone sophorolipid and the application thereof in preparing medicine for preventing and curing liver cancer, lung cancer, esophagus cancer, stomach cancer and breast cancer. Tests show that the chemical compound has strong inhibition effect to HepG cell2 of liver cancer, A-549 cell of lung cancer, SGC7901 cell of stomach cancer, KYSE109 cell of esophagus cancer and MDA-MB-435 cell of breast cancer for people when the concentration is 50 mg/kg, provides foundation and approach for antineoplastic drug which resists various tumors, has less toxic side effects and obvious effects, and has vital meaning.
CN101053557A Noradrenaline bitartrate medicine composition frozen dried powder injection The invention relates to a medicine and preparation field, in detail, a injection of anti-shock blood vessel medicine combination bitartrate noradrenaline freeze-dry powder injection and its producing method. The inventive bitartrate noradrenaline freeze-dry powder injection is composed of bitartrate noradrenaline and medical acceptable carrier component, wherein said medical acceptable carrier is selected from one of more mannitol, L-arginine, low molecule dextran, cyclodextrin, soluble amylum, carbohydrate matter, sodium chloride, chlorobenzoic acid, amino acid matter or fibrous matter, preferred mannitol and L-arginine with a content of 1-50mg, preferred 1mg, 2mg, 5mg, or 10mg.
US6852736 Phenoxypropanolamines, preparation and therapeutic use thereof The invention concerns phenoxypropanolamines of formula (I) in which R1 represents a hydrogen, a group —S(O)z—(C1-C4)alk-R′, (R′ being H, phenyl or (C1-C4)alkoxy), —NHSO2—(C1-C4)alk or NHCO(C1-C4)alk; m and n are each independently 0, 1 or 2; R2 and R3 independently represent a hydrogen, a (C5-C6)alkyl, (C3-C6)cycloalkyl, (C1-C4)alkoxy, hydrogen(C1-C4)alkoxy-(C1-C4)alkyl, mono- or di(C1-C4)alkamino(C1-C4)alkyl, pyrrolidino(C1-C4)alkyl, phenylamino or (C2-C4)alkenyl group, an aromatic or heteroaromatic group optionally substituted with a group R4, an aralkyl or heteroaralkyl group optionally substituted with a group R4, R2 and R3 can also together constitute a saturated or unsaturated ring of 3 to 8 atoms possibly bearing a (C1-C4)alkyl, amino (C1-C4)alkyl, carbamoyl or benzyl substituent; R4 represents a hydrogen or a halogen, or a group —CO(C1-C4)alk or a group —NHSO2—(C1-C4)alk; a group (C1-C4)alk, a group (C1-C4)alkoxy, a halogen, —COOH, —COO(C1-C4)alk, —CN, —CONR3R4, —NO2, —SO2NH2 or —NHSO2(C1-C4)alk; z is 1 or 2; and the salts or solvates thereof. The compounds have agonist activity toward β-3 adrenergic receptors.
US7189731 2-amino-6-oxy-substituted pyrido[3,4d]pyrimidine derivatives; treating arthritis, Crohn's disease, Alzeihmer's disease, adult respiratory distress syndrome, chronic obstructive pulmonary disease, asthma, stroke, sepsis, myocardial infarction, and spondylitis. Compounds having the formula (I) or (II), are useful as p38 kinase inhibitors, wherein R is an optionally substituted alkyl, cycloalkyl, or aryl; R6 is hydrogen or lower alkyl; R7 is hydrogen or a non-interfering substituent, and Q is a non-aromatic moiety as defined in the specification.
WO2007088704A1 Preventive/remedy for urinary calculosis A preventive/remedy for urinary calculosis which comprises L-aldonic acid, a salt thereof or a lactone compound thereof as the active ingredient.
CN101810622A Composition containing cefmetazole sodium The invention discloses a composition containing cefmetazole sodium, which is characterized in that the ratio of the cefmetazole sodium to mezlocillin sodium in the mixture is (1-5):1, based on the weight; the optimal ratio of the cefmetazole sodium to the mezlocillin sodium in the mixture is 3:1, based on the weight; and the ratio of the mixture of the cefmetazole sodium and the mezlocillin sodium to poloxamer is 50:1, based on the weight. By combining the cefmetazole sodium and the mezlocillin sodium, the invention greatly improves the antibacterial activity of the medicament, so that the antimicrobial spectrum is wider and the curative effect of the medicament is better.
CA2215350C Transforming growth factor alpha hii The present invention discloses transforming growth factor alpha HII polypeptides and polynucleotides encoding such polypeptides. Also provided is a procedure for producing such polypeptides by recombinant techniques and therapeutic uses of the polypeptides which include stimulating wound healing, treating neurological disorders, treating ocular disorders, treating kidney and liver disorders and stimulating embryogenesis and angiogenesis. Also disclosed are antagonists against such polypeptide and their use as a therapeutic to treat neoplasia. Also disclosed are diagnostic assays for detecting altered levels of the polypeptide of the present invention and mutations in the nucleic acid sequences which encode the polypeptides of the present invention.
CN101429174B Piperazine derivant with antineoplastic activity The invention discloses piperazine derivatives with anti-tumor activity, which have a structure as right, in the formula, when X is C=O, R is H or -CH3; and when X is -CHOH or -CH2, R is H. The compounds are obtained by using carvone as an initial raw material through chlorination reaction, condensation reaction, sodium borohydride reduction and Huang Min-lon reduction reaction. In vitro experiments show that the compounds have stronger propagation inhibiting effect on a cancer cell strain Lncap of human pancreas, are potential anti-tumor medicaments, and have application to preparing anti-tumor pharmaceutical preparations.
WO2009106019A3 Chemical compounds having antiviral activity against dengue virus and other flaviviruses The invention relates to the use of chemical compounds obtained in silico for the preparation of pharmaceutical compositions for attenuating or inhibiting dengue virus infection, in particular by interference with or modulation of the multiple steps of the viral replication cycle associated with the arrival of the virus in the target cells and the assembly of the progeny virions. The invention also relates to the use of said pharmaceutical compositions for the prophylactic and/or therapeutic treatment of infection caused by the four dengue virus serotypes and by other flaviviruses.
EP1592661A2 Cyclopropyl beta-amino acid derivatives This invention relates to novel cyclopropyl β-amino acids derivatives of the formula (I) wherein R1 through R4 are defined as in the specification, pharmaceutical compositions containing them and their use for the treatment of various central nervous system and other disorders. The cyclopropyl β-amino acids derivatives of this invention exhibit activity as alpha2delta ligands (α2δ ligands). Such compounds have affinity for the α2δ subunit of a calcium channel.
WO2010078730A1 Preparation of ginsenoside-rd propylene glycol aqueous solution and new use thereof in anti-inflammation, immunosuppression and anti organ-graft rejection The present invention provides preparation of ginsenoside-Rd propylene glycol aqueous solution and new use thereof in anti-inflammation, immunosuppression and anti organ-graft refection. The present invention provides a ginsenoside-Rd solution and preparation method thereof, said solution is prepared by adding ginsenoside-Rd to propylene glycol aqueous solution comprising 50-100%(v) propylene glycol, the content of ginsenoside-Rd is 1-100mg/ml solution, wherein the standard of the volume percentage is the bulk volume of propylene glycol aqueous solution. Furthermore, the present invention provides a medical composition of solution of the present invention and preparation method thereof, and the use of ginsenoside-Rd or ginsenoside-Rd solution of the present invention in manufacture of medicaments for anti-inflammation, immuneosuppression and/or anti organ-graft rejection.
CA2386549C Polymorphic b form of 3-(cyclopropylmethoxy)-4-[4-(methylsulfonyl)phenyl]-5,5-dimethyl-5h-furan-2-one This invention is related to a polymorphic B Form of 3-(cyclopropylmethoxy)-4-[4-(methylsulfonyl)phenyl]-5,5-dimethyl-5H-furan-2-one characterized by the above parameters (I).
US7713999 Thrombin receptor antagonists Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond, n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1-C6)alkyl, (C3-C8)cycloalkyl, —OH, (C1-C6)alkoxy, R27-aryl(C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms, Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
CA2391832C Oral dosage forms The invention relates to oral dosage forms with controlled total-release of an active substance. Said active substance is present in the form of at least two different salts that are present in the dosage form in a solid state of aggregation and that release said active substance in vitro differently.
CN101891618B 2-[(2,3,4-trialkoxy-6-acyl) phenyl] acetic ester as well as preparation method and application thereof The invention discloses 2-[(2,3,4-trialkoxy-6-acyl) phenyl] acetic ester as well as a preparation method and application thereof and relates to an organic micromolecule compound. The preparation method comprises the following steps of: converting 2,3,4-trialkoxy benzaldehyde 1 used as a raw material into 3-(2,3,4-trialkoxy) phenylpropionic acid 2 by using Meldrum acid; under the action of polyphosphoric acid, carrying out intramolecular acylation on the 3-(2,3,4-trialkoxy) phenylpropionic acid 2 to obtain corresponding idenone hydride 3; carrying out an addition reaction on the idenone hydride 3 with a Grignard reagent and dewatering into indene hydride 4 by using acid; treating the indene hydride 4 by using osmium tetroxide to obtain dihydroxyl indene hydride 5; oxidizing the dihydroxyl indene hydride 5 respectively by using sodium periodate and sodium chlorite to obtain 2-[(2,3,4-trialkoxy-6-acyl) phenyl] acetic acid 7; and finally, reacting the 2-[(2,3,4-trialkoxy-6-acyl) phenyl] acetic acid 7 with anhydrous alcohol to obtain the 2-[(2,3,4-trialkoxy-6-acyl) phenyl] acetic ester 8 as the target product in the presence of thionyl chloride. The 2-[(2,3,4-trialkoxy-6-acyl) phenyl] acetic ester can activate monophosphate activated protein kinase and is useful for preparing anti-diabetic medicaments.
US20080038365 TRPC6 involved in glomerulonephritis Focal and segmental glomerulosclerosis (FSGS) is a kidney disorder of unknown etiology and up to 20% of patients on dialysis have this diagnosis. A large family with hereditary FSGS carries a missense mutation in the TRPC6 gene on chromosome 11q, encoding the ion channel protein Transient Receptor Potential Cation Channel 6. The missense mutation is a P112Q substitution, which occurs in a highly conserved region of the protein, enhances TRPC6-mediated calcium signals in response to agonists such as angiotensin II, and alters the intracellular distribution of TRPC6 protein. Previous work has emphasized the importance of cytoskeletal and structural proteins in proteinuric kidney diseases. Our findings suggest a novel mechanism for glomerular disease pathogenesis.
CN102526092A Application of polysaccharide in medicament for treating or preventing primary cerebral infarction The invention relates to novel application of the medical effect of polysaccharide, in particular to application of polysaccharide in a medicament for treating or preventing primary cerebral infarction. Drug administration before a cerebral infarction model indicates that the polysaccharide has good prevention effect on the cerebral infarction (the inhibition ratios to the cerebral infarction areas are respectively 15 percent, 72 percent and 90 percent if dosages are 30, 60 and 100mg/kg); and drug administration after the cerebral infarction model indicates that the polysaccharide has good treatment effect (the inhibition ratios to the cerebral infarction areas are respectively 75 percent and 96 percent if dosages are 60 and 100mg/kg). No matter drug administration is carried out before or after the cerebral infarction, the polysaccharide has remarkable inhibition effect on the cerebral infarction area, which indicates the clinical treatment practicability of polysaccharide in cerebral infarction treatment. The polysaccharide can be used as a prevention medicament and a treatment medicament, so that the cure rate and survival rate of cerebral infarction can be improved, and the current situation of high disability rate and high fatality rate can be changed possibly.
CA2180816C 6-dimethylaminomethyl-1-phenyl-cyclohexane compounds as pharmaceutical active ingredients 6-dimethylaminomethyl-1-phenyl-cyclohexane compounds, methods of preparing them and the use of these compounds in drugs are described.
US20090239938 Preventive/remedy for arteriosclerosis A scavenger receptor A expression down-regulator and a drug for preventing or treating arteriosclerosis which contain, as the active ingredient, a C-terminal globular domain of adiponectin, adiponectin, or a gene encoding the domain or adiponectin. According to the present invention, there is provided a preventive or therapeutic agent capable of directly preventing intimal thickening, which constitutes an essential feature of arteriosclerosis. This effect can be attained through arresting the onset and development of arteriosclerosis by reducing the expression level of scavenger receptor A in arterial walls and preventing lipid buildup in macrophages.
CA2384624C Dosage forms and methods for providing effective reboxetine therapy with once-a-day dosing Dosage forms and methods for providing sustained release of reboxetine are provided. The sustained release dosage forms provide therapeutically effective average steady-state plasma reboxetine concentrations when administered once per day. This once-a-day dosing regimen results in only one peak plasma reboxetine concentration occurrence in each 24 hour period. In addition, the peak plasma reboxetine concentration occurs at a later time following dose administration and exhibits a lesser magnitude than the peak plasma reboxetine concentration that occurs following administration of reboxetine in an immediate-release dosage form.
CN103356504A 4-Amino-2-trifluoromethylphenylretinoate self-microemulsion and preparation method thereof The invention relates to a technology of improving the in-vitro dissolution of an indissolvable medicament, discloses a self-microemulsion, and especially discloses an ATPR (4-Amino-2-Trifluoromethyl Phenyl Retinoate) self-microemulsion and a preparation method thereof. The ATPR self-microemulsion is characterized by being prepared from the following components by weight percent: 0.1-20% of ATPR, 1-30% of oil phase, 40-85% of surfactant and 1-40% of cosurfactant. The self-microemulsion and the preparation method provided by the invention have the following beneficial effects: the solubility of the medicament is improved by the ATPR self-microemulsion drug release system, the medicament is dissolved in oil drops and thus protected and the stability of the medicament in vivo is improved, the surfactant is capable of changing the liquidity of the cell membrane and improving the membrane permeability of the medicament, so that the in-vivo absorption of the medicament is increased and the relative bioavailability of the medicament is improved. Besides, the solid self-microemulsion is capable of improving the phenomena of softening and oil leakage of the traditional soft capsules and enhancing the stability of the preparation.
WO2013034755A1 Triazolopyrazine derivatives and their use for treating neurological and psychiatric disorders The present invention is directed to triazolopyrazine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psychiatric disorders.
EP1944295A1 Non-racemic mixtures of (R)-N-piperidinyl-5-(4-chlorophenyl)1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide and (S)-N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide The present invention relates to non-racemic mixtures of (R)-N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide and (S)-N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1 H-pyrazole-3-carboxamide, methods for their preparation, medicaments comprising the mixtures as well as use for the preparation of a medicament for the treatment of humans and animals and the use of (S)-N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide in the prophylaxis and/or treatment of dyslipidaemia and other metabolic disturbances that result from the excessive consumption of highly palatable macronutrient food sources.
WO2007054294A1 Pyrazolo-pyrimidine derivatives as anti-inflammatory agents The present invention is directed to compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation and/or allergic conditions.
US20120165387 General composition framework for ligand-controlled RNA regulatory systems The invention provides an improved design for the construction of extensible nucleic acid-based, ligand-controlled regulatory systems, and the nucleic acid regulatory systems resulting therefrom. The invention contemplates improving the design of the switches (ligand-controlled regulatory systems) through the design of an information transmission domain (ITD). The improved ITD eliminates free-floating ends of the switching and the competing strands, and localizes competitive hybridization events to a contiguous strand of competing and switching strands in a strand-displacement mechanism-based switch, thereby improving the kinetics of strand-displacement. The improved regulatory systems have many uses in various biological systems, including gene expression control or ligand-concentration sensing.
WO2011032203A1 Contact lens disinfecting solutions This invention relates to ophthalmic disinfecting and preserving compositions. More particularly, this invention relates to multi-purpose disinfecting solutions [MPDS] suitable for use in or with storage cases for treating multiple-use contact lenses and/or for preserving, disinfecting or packaging of contact and other ophthalmic lenses.
CN101322714A Anti-herpes simplex virus I-form medicament composition and uses thereof The invention relates to a pharmaceutical composition with dammarane-type tetracyclic triterpene compound as an active component and an application thereof to the pharmaceutical field. Panax notoginseng is separated to obtain three dammarane-type tetracyclic triterpene compounds as shown in the following structural formula, in vitro pharmacological experiments show that the pharmaceutical composition has good in vitro inhibitory activity for herpes simplex virus type I and can be applied to the preparation of medicines for resisting herpes simplex virus type I and is used for treating herpetic keratitis, encephalitis, pneumonia, ulcerative stomatitis, blister and the like caused by herpes simplex virus type I.
CN101134723A Gallic acid and divalent metal ionic compound and preparation method and application thereof The present invention relates to organic metal complex, and discloses six kinds of complex of gallic acid and bivalent metal ion and their preparation process and application. The complexes are prepared through the complex reaction of gallic acid and bivalent metal ion. After entering into organism, the complexes may release metal ions, Ca, Mg, Zn, ferrous iron, Cu and Mn, for ingestion while the liberated gallic acid produces antiviral, antitumor, antimutation, antioxidizing and other health functions. Compared with similar compounds, the present invention has the advantages of high absorption rate, low toxicity and low cost.
WO2010078659A1 Compositions and methods for nutritional prevention and treatment of alzheimer's-associated conditions The present invention provides nutraceutical compositions containing an aluminum-blocking component and a calcium-enhancing (and magnesium-enhancing) component, and optionally additional nutrients that address the harmful effects of aluminum on the brain. The compositions find use in nutritional methods for treating and/or preventing Alzheimer's and related conditions. The methods generally involve oral administration of the nutraceutical composition to an individual having or at risk for Alzheimer's.
CN102964328A Isopentene isoflavanone compound as well as preparation method and application of compound The invention relates to a natural medicine, and in particular relates to a novel isoflavanone isoflavanone compound in wild peanuts as well as a preparation method and application of the compound. The novel isoflavanone isoflavanone compound provided by the invention has a structural formula shown in a formula (I). The preparation method comprises the following steps of: a, crushing; b, refluxing and extracting; c, concentrating; d, extracting; and e, separating. The novel isoflavanone isoflavanone compound shown in the formula (I) has a remarkable inhibition function to a human cervical carcinoma, human chronic myeloid leukemia or human acute myelogenous leukemia cell strain, has a better anti-cancer activity, and can be used as an anti-cancer active component or lead compound. The novel isoflavanone isoflavanone compound can be a natural organic compound, is wide in raw material source, is simple in preparation process, is high in purity, is easily realized in subsequent industrialized production, is used for preparing a medicament for preventing or treating tumors, and is used for clinically treating human cervical carcinoma, human chronic myeloid leukemia or human acute myelogenous leukemia.
WO2014001228A1 Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors The present invention provides difluoro-cyclopentaoxazinyls and difluoroenzooxazinyls of formula (I) having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
US20090202552 Gene expressed in prostate cancer and methods of use A new polypeptide is disclosed that is specifically detected in the cells of the prostate, termed Novel Gene Expressed in Prostate (NGEP). Polynucleotides encoding NGEP are also disclosed, as are vectors including these polynucleotides. Host cells transformed with these polynucleotides are also disclosed. Antibodies are disclosed that specifically bind NGEP. Methods are disclosed for using an NGEP polypeptide, an antibody that specifically binds NGEP, or a polynucleotide encoding NGEP. Assays are disclosed for the detection prostate cancer. Pharmaceutical compositions including an NGEP polypeptide, an antibody that specifically binds NGEP, or a polynucleotide encoding NGEP are also disclosed. These pharmaceutical compositions are of use in the treatment of prostate cancer.
US20090291965 Histone Deacetylase Inhibitors With Aryl-Pyrazolyl-Motifs The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.
US20090036461 Use of Azabicyclo Hexane Derivatives The present invention provides a new use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate salt thereof: wherein: G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxyl, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3I s C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; in the manufacture of a medicament for the treatment of a somatoform disorder such as body dysmorphic disorder or hyperchondriasis, bulimia nervosa, anorexia nervosa, binge eating, paraphilia and nonparaphilic sexual addictions, Sydeham's chorea, torticollis, autism, a movement disorder including Tourette's syndrome; and in the manufacture of a medicament for the treatment of premature ejaculation.
WO2006030941A1 Simultaneous use of sulfonamide-containing compound and angiogenesis inhibitor A pharmaceutical composition comprising a sulfonamide-containing compound combined with an angiogenesis inhibitor.
US20110015196 Lupeol-type triterpene derivatives as antivirals The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
US20100216808 Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
EP2737902A1 Compositions comprising cimetidine and n,o-carboxymethyl chitosan for the prevention and therapy of pathologies of the skin and the mucous membranes and in the odontostomatological field Topical compositions comprising an H2 receptor antagonist and cimetidine and a chitosan soluble derivative in admixture with suitable carriers and excipients.
US20110250296 Reverse vitamin k effect via photodynamic oxidation targeted at vascular endothelium, fibrin and blood platelets A formulation or preparation for treating and preventing arterial and venous thrombi is provided. This preparation includes a non-metal containing photodynamic dye and a fat soluble vitamin. A method of administration for treatment and prophylaxis of arterial and venous thrombi is also provided. This method includes steps of: combining a non-metal containing photodynamic dye and a fat soluble vitamin; combining the non-metal containing photodynamic dye and fat soluble vitamin with a sodium solution; and administering the combination of non-metal containing photodynamic dye, fat soluble vitamin, and sodium solution as an intravenous drip.
EP1390027B1 Composition comprising demethylcantharidin in combination with platinum-containing anticancer agents and use thereof The invention provides a pharmaceutical composition for inhibiting cisplatin, carboplatin or oxaliplatin-sensitive and resistant tumorous cells comprising a combination of demethycantharidin with a platinum-containing anticancer agent and a use thereof. The invention also discloses synergistic effect of demethycantharidin or pharmaceutically acceptable derivative thereof in combination with platinum-containing anticancer agents in inhibiting cisplatin, carboplatin or oxaliplatin-sensitive and resistant tumorous cells.
CN1730479A Aloe dihydro-coumarin and its separation method and uses Disclosed is a process for separating aloe dihydrocoumarin and its use, wherein the separation process comprises extracting the aloe concrete with acidic chloroform, concentrating the extract and dissolving with aqueous solution of ethanol, then carrying out solvent distribution in sequence with n-hexane, chloroform and alcohols, concentrating the chloroform portion, passing through column chromatography, eluting multitime, thus obtaining the pure compound having oxidation resistance, immune regulation action and antineoplastic activity.
EP2030612A1 Pharmaceutical composition for treating burns (variants) and a method for the production thereof (variants) The invention relates to medicine, in particular to soft medicinal agents for external application (ointment, gels, emulsions, liniments) and can be used for treating thermal, solar and chemical burns of human beings and animals. The inventive pharmaceutical composition for treating burns is embodied in the form of a gel and contains an active substance N -(β-oxyethyl)-4, 6-dimethyldihydropyrimedon-2 (xymedon), a gel former, a moisture retaining agent and distilled water. The gel former can be embodied in the form of sodium, carboxymethylcellulose, sodium alginates or the mixture thereof and the moisture retaining agent is embodied in the form of glycerin. In the other embodiments, additionally to xymedon, the composition can contain an active substance in the form of silver nitrate or silver nitrate and sodium sulphacyl or levomycetin and succinic acid. The tests have proved the high efficiency of said composition, which meets all the medical and biological requirements of modem medicinal agents used for treating burns and wounds. The pharmaceutical composition is embodied in the form of a gel and can be used as highly efficient regenerating, wound-healing and micro-circulation improving means for treating infected burn wound.
WO2011087652A1 Tropinone benzylamines as beta-tryptase inhibitors The present invention discloses and claims a series of substituted tropinone benzylamines of formula (I). More specifically, the compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted tropinone benzylamines.
WO2007036306A1 2-aminoethoxyacetic acid derivatives and their use in treating thromboembolic disorders The present application relates to new 2-aminoethoxyacetic acid derivatives, to processes for preparing them, to their use in the treatment and/or prophylaxis of diseases, and also to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.
CN102670581A Application of alpha-mangostin for prevention and treatment of diabetes mellitus The invention provides an application of alpha-mangostin for prevention and treatment of diabetes mellitus. Alpha-mangostin can be used for decreasing blood glucose of diabetics, increasing glucose tolerance and improving symptoms of polydipsia, polyuria, polyphagia, emaciation and thirsty of the diabetics, can also be used for lowering high-fat-diet-induced obesity mouse total cholesterol content, has a cholesterol lowering effect, is capable of improving abnormality of the high-fat-diet-induced mouse glucose tolerance, and has functions of preventing and delaying obese patients from getting diabetes mellitus.
WO2009137251A3 Cysteine and cystine bioisosteres to treat schizophrenia and reduce drug cravings The present invention provides cysteine and cystine bioisosteres for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing such bioisosteres and methods of using the bioisosteres for treatment of schizophrenia and drug addiction.
WO2009113950A1 Therapeutic combinations of (a) an antipsychotic and (b) an alpha-4/beta-2 (a4b2)-neuronal nicotinic receptor agonist The present invention relates to a combination of (a) an antipsychotic and (b) an alpha4/beta2 (α4β2)-neuronal nicotinic receptor agonist, which is 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane. The invention further relates to pharmaceutical compositions comprising said combination and to the use of the combination in therapy. The invention further relates to a kit comprising the combination and use of said kit in therapy.
CN102379851A Preparation method of cobamamide lyophilized preparation for injection The invention discloses a preparation method of cobamamide lyophilized preparation for injection. The preparation method of cobamamide lyophilized preparation for injection comprises following steps that medicine components include, by weight, 0.5-1 parts of cobamamide and 30 parts of mannitol; the cobamamide and the mannitol are weighed under a red light lamp with the illumination intensity of 20 lux to 50 lux, are added into water filled with inert gas and are stirred so as to be dissolved, 0.1% to 0.2% of activated carbon is added into mixture of the cobamanide, the mannitol and the water, and then mixture of the activated carbon, the cobamanide, the mannitol and the water is finely filtered, charged separately, filled with inert gas to be protected and then is lyophilized. Chemical stabilizing agent such as bacteriostat, complexing agent, opacifier and the like is not used in the preparation method. The preparation method not only is convenient for work of operators, but also can prevent stability of the quality of products from being affected due to inappropriate light shielding methods, and simultaneously, stability of the products is improved.
US20080213256 Less Immunogenic Binding Molecules The present invention provides a bispecific binding molecule, wherein said molecule comprises or consists of at least two domains whereby one of said at least two domains specifically binds to/interacts with the human CD3 complex and said domain comprises an amino acid sequence of an antibody derived light chain, wherein said amino acid sequence is a particularly identified amino acid sequence comprising specific amino acid substitutions, and a second domain is or contains at least one further antigen-interaction-site and/or at least one further effector domain. The invention further provides nucleic acid molecules encoding the bispecific binding molecules of the invention, vectors comprising said nucleic acid molecules and host cells transformed or transfected with said vectors. Moreover, the invention concerns a method for the production of bispecific binding molecules of the invention and compositions comprising the bispecific binding molecules of the invention, the nucleic acid molecules of the invention or the host cells of the invention.
CN101292985A Levofloxacin Lactate freeze-dried injection and preparation method thereof The invention discloses a lactic levofloxacin freeze-dried powder injection and a preparation method thereof. The existing lactic levofloxacin freeze-dried powder injection is easily to be influenced by polyvalent metal ions to have shortcomings such as color difference in one batch, the product quality is reduced. The freeze-dried powder injection comprises the lactic levofloxacin, stabilizer and excipient. The weight proportion of the lactic levofloxacin and the stabilizer is 30:1-2:3 and the weight proportion of the lactic levofloxacin and the excipient is 1:5-5:1. The method can effectively reduce the influence of polyvalent metal ions in the preparation process and can improve the quality of products.
CN101422544A Haifei capsule formulation with weight reduction function and preparation method thereof The invention relates to a prescription and the preparation method of a slimming drug, i.e., Haifei capsule which consists of semen cassiae, tuckahoe, thallus eckloniae, chitosan, L-carnitine, konjaku powder, spirulina powder and pearl, and the corresponding weight proportion (parts by weight) of each component is as follows: 6 to 30, 6 to 30, 5 to 25, 2 to 15, 2 to 20, 2 to 16, 2 to 10 and 0.1 to 2. The preparation method comprises the following steps of: crushing the pearl; screening the L-carnitine, chitosan and spirulina powder by a sieve with 80 screen meshes; decocting the semen cassiae, tuckahoe, thallus eckloniae in water for three times, merging, filtering and condensing the decocting liquid, adding the medicine powder and konjaku powder which are mixed and then packed in capsules. The Haifei capsule has effects of clearing away impurity and promoting diuresis, invigorating the spleen and removing stagnated feed, relaxing bowel, supplementing the trace elements needed by human body, enhancing gastrointestinal peristalsis, reducing fat absorption and dispersing redundant grease in organism, thereby achieving the purpose of controlling weight reasonably and reducing fat excessive accumulation.
US7732463 such as 4-[2-(4-Chloro-phenylsulfanyl)-5-trifluoromethyl-phenyl]-piperidine, used as antidepressants and anxiolytic agents; treatment of panic and obsessive compulsive disorders The invention provides compounds represented by the general formula (I) wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
US20120270899 Compositions and Methods for Treating Cardiovascular Diseases The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions.
US20100003216 HCV NS-3 Serine Protease Inhibitors Compounds of the formula where the variables are as defined in the specification inhibit the NS3 protease of flavivirus sych as hepatitis C virus (HCV). The compounds comprise a novel linkage between a heterocyclic P2 unit and those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.
WO2004089417A9 Drug-enclosing multilayer structure particulate and process for producing the same A drug-enclosing multilayer structure particulate comprising a calcium carbonate compound particulate enclosing a biologically active substance wherein occasionally ions of at least one metal selected from among zinc, magnesium, iron and copper are contained and, superimposed on the surface thereof, a coating of calcium phosphate porous material and/or biopolymer.
CN102048684A Method for preparing rocuronium bromide injection The invention discloses a method for preparing rocuronium bromide injection, which comprises the following steps of: making each 50,000ml of injection contain the following components by weight: 20 to 70.0g of rocuronium bromide, 1 to 20.0g of sodium acetate and 0.5 to 2.0g of sodium chloride; cooling water for injection to room temperature; adding acetic acid-sodium acetate buffer solution, and mixing uniformly; dissolving the sodium chloride and the rocuronium bromide; regulating the pH value of the solution to be 4.0 by using 1mol/L acetic acid; adding active carbon, removing carbon, filtering, and filtering to remove bacteria through a 0.22 mu m microporous filtering film; and filling and sterilizing. The method is simple in process, and the product quality is stable.
WO2006125887A1 5h-pyrido[4,3-b]indole derivative compounds and uses thereof as medicine for treating polyglutamin neurodegenerative diseases The invention concerns the treatment of neurodegenerative diseases. More particularly, it concerns a family of compounds derived from 5H-pyrido [4,3-b] indole for which a neuroprotecting activity has been shown. The invention concerns those novel products, their synthesis methods as well as certain likewise novel synthesis intermediates. The invention also concerns compositions comprising the compounds of said family, the use of said compounds as drugs, in particular for preparing a medicine for treating polyglutamin neurodegenerative diseases.
WO2006034567A1 Use of compositions comprising farnesyl dibenzodiazepinones for treating neoplastic cells and conditions This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms using the farnesylated dibenzodiazepinone compound of Formula I. The invention includes pharmaceutical compositions comprising the compound of Formula I:
CN103006561A Lipofectin nanometer silver gel and preparation method thereof The invention relates to a lipofectin nanometer silver gel and a preparation method of the lipofectin nanometer silver gel. The lipofectin nanometer silver gel is prepared from the following raw materials in parts by weight: 1.5 to 4.5 parts of soya bean lecithin and cholesterol, 1 to 9 parts of chitosan, 1 to 20 parts of glycerol, 0.1 to 2 parts of oleum menthae, 30 to 70 parts of acetum, 20 to 60 parts of nanometer silver solution, and the balance of deionized water. According to the preparation method, the nanometer silver is prepared into lipofectin, most of the nanometer silvers are encapsulated in a bilayer formed by the lipofectin, and therefore the stability of the nanometer silver can be improved; and the proper macromolecular optimum formula is adopted to prepare the gel, thus the convenience is provided for paving medicine on the skin. The prepared preparation has the advantages of being stable in medicine release rate, convenience in medicine paving, low in frequency of using the medicine, free from toxicity and stimulation and high in compliance of a user, and can be used for preventing and treating skin intolerance caused by various pathogenic microorganisms.
CN102516301A Therapeutic wogonin derivate The invention provides a wogonin derivate, and a preparation method and an application thereof. The structural hydroxyl groups are chemically modified, thereby obtaining the wogonin derivate. The wogonin derivate can be applied to the medicinal composition and can be used for producing the medicines for treating hepatitis B and leukemia.
CN1943572A Oral natural plant formula with anti-sunlight function A making up prescription of natural plant taking orally for sunscreen, its main ingredients are catechin, vitamin, vitamin E, catechin is of anti oxygenation, plus vitamin C is capable of preventing photo-aging and stimulating multiplication of skin collagen, therefore appropriate being element for long term skin protection.
WO2010143825A2 Anti-arthritic agent using cyathula officinalis The present invention is related to the inventive compositions comprising an extract of Cyathula officinalis or sesquiterpene isolated therefrom, show potent anti-inflammatory effect through various experiments, therefore, it can be used as the effective and safe therapeutics or health food for treating and preventing a disease in a subject mediated by MMP-13, preferably, arthritic disease.
CA2338186C Tumor necrosis factor-gamma Human TNF-gamma-alpha and TNF-gamma-beta polypeptides and DNA (RNA) encoding such polypeptides and a procedure for producing such polypeptides by recombinant techniques is disclosed. Also disclosed are methods for utilizing such polypeptides to inhibit cellular growth, for example in a tumor or cancer, for facilitating wound-healing, to provide resistance against infection, induce inflammatory activities, and stimulating the growth of certain cell types to treat diseases, for example restenosis. Also disclosed are diagnostic methods for detecting a mutation in the TNF-gamma-alpha and TNF-gamma-beta nucleic acid sequences or overexpression of the TNF-gamma-alpha and TNF-gamma-beta polypeptides. Antagonists against such polypeptides and their use as a therapeutic to treat cachexia, septic shock, cerebral malaria, inflammation, arthritis and graft-rejection are also disclosed.
US7304071 stroke, inflammatory disorders, autoimmune diseases such as SLE lupus and psoriasis, proliferative disorders such as cancer, and conditions associated with organ transplant; 2-amino-4-(p-aminocarbonyl)phenyl-substituted pyrimidine compounds Described herein are compounds that are useful as protein kinase inhibitors having the formulae I and V: or a pharmaceutically acceptable salt thereof, wherein Ring B, Z1, Z2, U, T, m, n, p, Q, Q′, R1, R2, Rx, R3, and R6 are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including stroke, inflammatory disorders, autoimmune diseases such as SLE lupus and psoriasis, proliferative disorders such as cancer, and conditions associated with organ transplantation.
US7985587 Methods of culturing dermal papilla cells The invention features methods of promoting hair growth in a subject. The methods include inducing or mimicking the effects of Wnt promoted signal transduction, e.g., by increasing the level of Wnt protein or administering an agent which mimics an effect of Wnt promoted signal transduction, e.g., by administering lithium chloride. Methods of inhibiting hair growth are also provided.
CN101028257A Use of Teroo hydrochloride and its chemical analog in preparation of anti-liver fibrotic medicine An application of the tiluoou hydrochloride and its chemical analog in preparing the medicines for preventing and treating hepatofibrosis is disclosed.
US20050154061 peroxisome-proliferator-activated receptor (PPAR)-delta agonist; 2-[4-[[[2-[(2,4-Dichlorophenyl)amino]-2-oxoethyl]cyclohexylamino]methyl]-2-methylphenoxy]-2-methylpropanoic acid; cardiovascular disorders, dyslipidaemias or restenosis; improves HDL/LDL cholesterol ratio; side effect reduction The present invention relates to novel substituted acetic acid derivatives, to processes for their preparation and to their use in medicaments, in particular as potent PPAR-delta-activating compounds for the prophylaxis and/or treatment of cardiovascular disorders, in particular dyslipidaemias and coronary heart diseases.
WO2012118309A2 Pyrazole derivatives, preparation method thereof, and composition for preventing and treating osteoporosis containing same The present invention provides a pyrazole derivative compound and pharmaceutically acceptable salts thereof. The compound of the invention is remarkably effective for preventing and treating osteoporosis.
CN101671278A Carbamic acid alkannin ester as well as preparation method and application thereof The invention discloses a carbamic acid alkannin ester as well as a preparation method and an application thereof. The preparation method comprises: 1mol of alkannin reacts with 1-2mol of isocyanate in methylbenzene at the reaction temperature of 80-100 DEG C for 10-15 hours, and column chromatography separation is carried out to obtain carbamic acid alkannin ester. The carbamic acid alkannin ester is used for preparing drugs with antitumor activity and drug resistance. The invention prepares the carbamic acid alkannin ester by the simple and easy method, and carries out inspection on the antitumor activity and drug resistance of the carbamic acid alkannin ester, finds that the carbamic acid alkannin ester has strong inhabiting effect to tumor cell lines, and proves that the carbamic acidalkannin ester has good drug resistance and is an antitumor drug with prospects.
CN1562017A Balofoxacin liquid preparation preparing method and its use A liquid Baluoshaxing for treating bacterial infection contains Baluoshaxing, acid as dissolving aid, and water.
CN103006652A Pharmaceutical composition capable of reducing blood pressure and blood fat simultaneously and preparation method of pharmaceutical composition The invention provides a pharmaceutical composition capable of reducing blood pressure and blood fat simultaneously and a preparation method of the pharmaceutical composition. The pharmaceutical composition is characterized in that amlodipine besylate and atorvastatin calcium are used as main medicines according to a combination proportion of 1: (1-10), and auxiliary materials comprise a filling agent, a disintegrating agent, a flow aid, a moistureproof agent and a lubricating agent. The preparation method comprises the following steps of: (1) drying the filling agent, and weighing the main medicines and the auxiliaries; (2) respectively screening the filling agent and the disintegrating agent by a 70-90-mesh sieve, and then mixing for later use; (3) mixing a half of spare mixed auxiliary material with amlodipine besylate to obtain a mixture, and jointly grinding the mixture, and screening the mixture by a 70-90-mesh sieve to obtain a ground material for later use; (4) jointly grinding the atorvastatin calcium and the rest spare auxiliary material to obtain a mixture, and screening the mixture by a 70-90-mesh sieve to obtain a ground material for later use; and (5) uniformly mixing the ground material of the amlodipine besylate and the atorvastatin calcium to obtain a mixture, and filling the mixture into capsules. The combination medicine disclosed by the invention has the effects of reducing blood pressure and blood fat; and the preparation method is scientific and reasonable, good in reproducibility, simple to operate and easy for mass production.
WO2009009529A1 Treatment of progressive neurodegenerative disease with ibudilast Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
US20070092499 Method for changing genetic properties of eukaryotic organism The invention provides a method for changing the genetic properties of an eukaryotic organism by suppression of expression of a target gene. Proposed method can be used in gene-therapy in medicine, agriculture, or industrial biotechnology. Genetic properties of an eukaryotic organism are changed by gene-specific silencing of a selected gene using small RNA molecules, that are complementary in a parallel orientation (pcRNAs) to mRNA of the selected gene; wherein pcRNAs are synthesized in vivo or in vitro on the artificial DNA sequence encoding pcRNA, said artificial DNA sequence possesses symmetrical nucleotide ordering (mirror inversion) in respect to the nucleotide sequence of the gene.
CN101696166A Preparation method for danshen root salvianolic acid A The invention discloses a preparation method for danshen root salvianolic acid A, which is characterized in that total phenolic acid in danshen root is converted into the salvianolic acid A by using a certain method so as to greatly improve the extraction efficiency of the salvianolic acid A. The danshen root salvianolic acid A is prepared into tablets, capsules, granules, soft capsules, pellets, pills and oral liquid. Pharmacological experiments show that the salvianolic acid A has good pharmacological effects.
CN1739568A Dietotherapeutic nutrient for preventing and treating adipose diabetes and its prepn process The dietotherapeutic nutrient for preventing and treating adipose diabetes consists of purine nucleotide, compound vitamin, compound trace elements, compound mineral matter, essential fatty acid oil and proper amount of edible cellulose as stuffing and hypoglycemic. The dietotherapeutic nutrient is used as main material or additive for food products and medicines for preventing and treating diabetes through balancing insulin and hyperglycemic hormone, repairing the functions of pancreatic island and kidney, preventing and treating complication and restoring normal synthesis and metabolism. The present invention has c-GMP, trace elements, etc. to regulate second messenger c-AMP amount, lift, activity and release time of hyperglycemic hormone, calcium carbonate to buffer and neutralize flavone and other acid matter and acid poisoning, potassium citrate to replenish potassium and to maintain acid-alkali and electrolyte balance. The dietotherapeutic nutrient has no toxic side effect and dependence.
US20100316695 Condensation products based on bicyclic or polycyclic aromatics or heteroaromatics The invention relates to a condensation product obtainable by reaction of a1) at least one bicyclic or polycyclic aromatic or heteroaromatic, where the bicyclic or polycyclic aromatic or heteroaromatic is substituted by at least one carboxyl group (—COOH), and where the carboxyl group can be present in salt form, a2) at least one carbonyl compound, a3) if appropriate at least one sulfonating agent, a4) at least one urea derivative, and a5) if appropriate at least one further aromatic or heteroaromatic, or a physiologically tolerable salt thereof.
US20100113417 Substituted Spiroamine Compounds Substituted spiroamine compounds corresponding to the formula (I) In which m, n, o, p, Q, r, s, t, R1, R2, R3, R4a, R4b, R5a, R5b, R6a, R6b, R7, R8, R9, R10 and R11 have defined meanings; a process for the preparation of such compounds, pharmaceutical compositions containing such compounds and the use of substituted spiroamines for the treatment or inhibition of pain and/or other conditions mediated by the bradykinin 1 receptor.
US20050014847 Ambroxol for the treatment of chronic nociceptive pain A method of treating chronic nociceptive pain, osteoarthritis, irritable bowel syndrome, fibromyalgia, visceral pain, or rheumatoid arthritis in a patient in need thereof, the method comprising administering to the patient ambroxol or a pharmacologically acceptable salt thereof.
CA2567836A1 Treatment with gemcitabine and an egfr-inhibitor The present invention provides a method for manufacturing a medicament for treating tumors or tumor metastases, characterized in that a therapeutically effective amount of an EGFR kinase inhibitor and gemcitabine is used, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase inhibitor and gemcitabine combination in combination with a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practising this invention is the compound erlotinib HCl (also known as TarcevaTM).
CN102365975A Disinfectant prepared from marine organisms The invention relates to a disinfectant prepared from marine organisms. The disinfectant prepared from marine organisms is suitable for being used in restaurants, hotels, hospitals, markets, banks, schools, kindergartens, homes, offices and journeys. The disinfectant prepared from marine organisms also can be utilized for remedy after hand washing in hospitals, nursing centers, child care centers, nosheries, kitchens and bathrooms, or can be utilized for skin wound disinfection and vulva cleaning. Therefore, the disinfectant prepared from marine organisms has a wide application range, is suitable for skin disinfection and sterilization for people working in all fields, can effectively control transmission of diseases such as typhoid, influenza, dysentery, pinkeye, gonorrhea and various skin diseases, has long-lasting sterilization and bacteriostasis effects, does not have toxic and side effects, and can moisten skin.
US20050181040 Progestagenic dosage unit The subject invention concerns a method of producing pharmaceutical dosage units for oral administration comprising a progestagenic compound which perorally exerts progestagenic activity equivalent to that of the progestagen desogestrel.
WO2014039421A1 Isotopologues of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4h)-yl) piperidine-2-6-dione and methods of preparation thereof Provided herein are deuterated isotopologues of 3-(5-amino-2-methyl-4- oxoquinazolin-3(4H)-yl)piperidine-2,6-dione, or enantiomers or mixtures of enantiomers thereof; or a pharmaceutically acceptable salt, solvate, cocrystal or polymorph thereof, and processes for making the same. Pharmaceutical compositions comprising the isotopes- enriched compounds, and methods of using such compounds are also provided.
WO2013002584A3 Combination of effective substances causing synergistic effects of multiple targeting and use thereof The present invention relates to a combination of effective substances causing synergistic effects of multiple targeting, and to uses thereof. More particularly, the present invention relates to a composition for a functional health food; to a cosmetic composition; to a pain alleviating composition; and to a composition for treating/preventing itching or atopic dermatitis, wherein each composition contains, as active ingredients, two or more substances selected from a group consisting of (a) an antagonist to a 5-HT2(5-hydroxtryptamine subtype 2) receptor; (b) an antagonist to a P2X receptor; and (c) any one of an agonist to a glycine receptor, an antagonist to a glycine transporter (GlyT), an agonist to a gamma-aminobutyric acid (GABA) receptor, and an antagonist to GABA transporter 1 (GABA1). The multi-targeting complex composition (specifically, natural product complex composition) has synergistic effects, and thus a treatment using a combination of individual substances may achieve increased biological effects from the mechanisms which the individual substances involve. Thus, the multi-targeting complex composition may not only remarkably alleviate pain but may also increase effects of: alleviating symptoms of skin diseases such as itching and atopic dermatitis; preventing or ameliorating depression; relaxation; skin pore reduction; ameliorating wrinkles; skin regeneration; skin health; skin condition recovery; whitening; preventing or ameliorating athlete's foot; scalp health recovery and regeneration; stimulation of hair growth; prevention of premature gray hair; improving teeth or ameliorating periodontal diseases; etc.
US6887895 Aminolyzing; alcoholysis; comprises acid catalysts; for treatment of tumors or inhibition of fungi The invention relates to pseudolaric acid-B derivatives of general formula (I), wherein (a) R1 is cyano, heterocyclyl, COXR′ or CON(R″)2, wherein X is O or NH, R′ is H, cycloalkyl, alkyl, heterocyclic alkyl or arylalkyl, each R″ is independently alkyl, cycloalkyl or heterocyclicalkyl; (b) R2 is H, alkylacyl, arylalkylacyl, arylacyl or heterocyclylacyl; (c) R3 is COXY, amino or halogen, wherein X is O or NH, Y is H, NH2, hydroxy, alkyl, cycloalkyl, heterocyclicalkyl, hetroatom-substituted alkyl, tertiary amino-substituted ammonioalkyl, aryl, arylalkyl or polyhydroxyalkyl. The invention also relates to processes for preparing such derivatives and antitumor or antifungal pharmaceutical compositions containing the same.
CN1951383A Stabilized medical and cosmetic composition containing catechin The invention relates to a stabilized catechin, pharmaceuticals of its derivatives and cosmetic compositions, wherein the constituents include anti-oxidizing agent 0.01-20 wt%, metal chelating agent 0.01-20 wt%, catechin or its derivatives 0.05-5 wt%, and right amount of water.
CN102755334A Medicine composition of cycloartenyl ferulate The invention discloses a medicine composition of cycloartenyl ferulate. The medicine composition solves the problem that the cycloartenyl ferulate cannot dissolve in water easily and contains cycloartenyl ferulate and polyoxyl stearate. Stable and water-soluble oryzanol medicine composition solution is obtained by adding the cycloartenyl ferulate into the molten polyoxyl stearate. The invention further discloses a preparation method and preparation application of the medicine composition of cycloartenyl ferulate.
CN101953810A Breviscapine pill The invention discloses a Breviscapine pill, which is prepared by the following steps of: smashing Breviscapine into fine powder for later use; further taking polyethylene glycol 4000 and polyethylene glycol 6000, heating and melting the polyethylene glycol 4000 and the polyethylene glycol 6000 in a water bath at 80-85 DEG C, adding the fine powder of Breviscapine and mixing uniformly; controlling the condensing temperature at 0-5 DEG C; and dropping at a temperature of 70-75 DEG C. The Breviscapine pill has outstanding bioavailability.
US7776899 Mixture of phentolamine mesylate, papaverine hydrochloride and alprostadil with buffer; injecting into penis Improved drug compositions and methods useful in the treatment of male erectile dysfunction. An optimized mixture of the drugs phentolamine mesylate, papaverine hydrochloride, and alprostadil in a buffer containing L-arginine and glycine is to be injected into the penile tissue to produce an erection in otherwise impotent men.
EP2240171A2 Inhibitors of carbonic anhydrase ix Novel radiopharmaceuticals that are useful in diagnostic imaging and therapeutic treatment of disease characterized by over expression of CA-IX comprise a complex that contains a sulfonamide moiety which Ls capable of binding the active catalytic site of CA- IX, and a radionuclide adapted for radioimaging and/or radiotherapy:
WO2012131080A1 Aminoquinoxaline derivatives for treatment of neurodegenerative diseases The present invention relates to compounds of formula (I) below: for which: - X represents a hydrogen atom, a halogen atom, a group NO2 or NH2, - R0 represents H or -CH2-C≡CH, and - R1 and R2 each represent, independently of one another, a hydrogen atom; a saturated or unsaturated, linear or branched hydrocarbon-based chain comprising from 1 to 10 carbon atoms; or an optionally substituted aryl group, and also the pharmaceutically acceptable salts thereof, the stereoisomers thereof or mixtures of stereoisomers thereof in any proportion, in particular for use thereof as a medicament, in particular in the treatment or prevention of neurodegenerative diseases, and also the processes for the preparation thereof and the pharmaceutical compositions comprising same.
CN102188427A Double-unit preparation containing simvastatin and niacin The invention provides double-unit preparation containing simvastatin and niacin, which are bilayer tablets or compound capsules containing two tablets. The double-unit preparation comprises a simvastatin unit and a niacin unit, wherein the two medicine-containing units are isolated. The simvastatin unit contains 5, 10 or 15 mg of simvastatin and a pharmaceutically acceptable excipient. The niacin unit contains 500, 750 or 1,000 mg of niacin, a sustained-release carrier, a bonding agent, a lubricating agent and another necessary pharmaceutically application excipient. The sustained-release carrier may be cellulose with high expansibility and gelling property or derivatives thereof. The double-unit preparation containing simvastatin and niacin can be used for preparing medicines for regulating blood fat.
CN1742747A Anti-cold nasal administration composition The present invention relates to a nasal medication composition for relieving common cold symptom and inhibiting common cold virus. Said composite is made up by using (by wt%) 0.1%-60% of pseudoephedrine hydrochloride, 0.2%-30% of chlorphenamine and 0.1%-75% of ribavirin.
EP2331142A2 Use of a truncated elf-5a1 polynucleotide to induce apoptosis in cancer cells The present invention relates to the combinatorial use of an siRNA targeted against an endogenous gene to knock out or knock down expression of the endogenous gene in a host and a delivery of a polynucleotide encoding the gene in a delivery vehicle/expression vector to the host to provide expression in the host of the protein encoded by the polynucleotide. The present invention also relates to a truncated form of eIF-5Al that is useful for inducing apoptosis and killing of cells, especially cancer cells in a mammal.
US20090221637 Solid-state salt argatroban formulations and methods for producing and using the same Argatroban formulations and methods of making and using the formulations are provided. In an embodiment, the present disclosure provides a solid-state salt formulation of argatroban. Upon reconstitution, the solid-state argatroban forms a solution that can be essentially free of particles and suitable for administration. The solid-state argatroban can be in a crystalline and/or amorphous form. The solid-state argatroban can be packaged in a sealed container that may be aseptically-filled to reduce the microbiological burden of the formulation. The solid-state argatroban can be reconstituted with a solution and administered to persons needing same.
WO2010125891A1 Estrogen-like agonist For the purpose of treating/preventing disorders or diseases associated with estrogen deficiency, an extract from a hypha of Agaricus blazei Murrill and a brefeldin A component are utilized.
CN1903148A Active endouterine contraceptive device made of composite material An active intra-uterine device (IUD) is prepared from the basic material (low-density polyethene or silicon rubber) and the active substance chosen from steroid hormone contraceptive, Cu particles and copper oxide particles through proportional mixing and blow moulding.
US20050163724 Contains steroidal anti-inflammatory drug, carrier (saccharides, sugar alcohols, amino acids), and water The present invention relates to powdery inhalant compositions, each of which contains a steroidal anti-inflammatory drug, a carrier and water and has a water activity at 25° C. of from 0.35 to 0.75. Each powdery inhalant composition according to the present invention is high in the delivery rate of its steroidal anti-inflammatory drug to an inhalation target site from the nasal cavities or oral cavity, that is, to the alveoli, the bronchioles, the bronchial tubes or the airway, and allows the steroidal anti-inflammatory to exhibit its superb therapeutic effects.
CN1559394A Compound prepn. for lowering blood-sugar, and its use A hypoglycemic medicine for treating diabetes and repairing the damaged beta-pancreatic island cells contains the natural amino acid (taurine, cysteine and methionine) and the biguaride medicine (dimethyl biguaride and phenylethyl biguaride).
WO2014087904A1 Agent for preventing or treating osteoclast-induced disease An osteoclast differentiation inhibitor, an osteoclast-induced bone resorption inhibitor, a bone regeneration promoting agent, and an agent for preventing or treating resorptive osteopathy, having as an active ingredient an α7 nicotinic acetylcholine receptor selective antagonist.
US20090162286 Phosphodiesterase 10 Inhibition as Treatment for Obesity-Related and Metabolic Syndrome-Related Conditions The present invention provides methods to decrease body weight and/or body fat in animals, e.g., in the treatment of overweight or obese patients (e.g., humans or companion animals), or as a means to produce leaner meat in food stock animals (e.g., cattle, chickens, pigs), methods to treat non-insulin dependent diabetes (NIDDM), metabolic syndrome, or glucose intolerance, in patients in need thereof by administering a PDE10 inhibitor (alone or in combination with another therapeutic agent), kits for the above-identified therapeutic uses, and methods of identifying PDE10 inhibitors for the above-described therapeutic uses.
WO2006050472A3 Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous and -phosphinic acids Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3aminopropylphosphinic acid, and analogs thereof, methods of making prodrugs of 3aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.
US7090832 Cooling agents, pharmaceutical compositions having cooling agents and processes for making and using same The invention pertains to cooling agents comprising N-substituted p-menthane-3-carboxamides, menthyl acetate and solubilizer, and methods for making the cooling agents. The invention also concerns pharmaceutical compositions comprising the cooling agents, including tablets, suspensions and liquid solutions having active pharmaceutical agents for treating upper gastrointestinal tract distress, and methods for treating upper gastrointestinal tract distress in humans.
US20090247479 Therapeutic Use of Methionine to Reduce the Toxicity of Aminoglycoside Antibiotics Methods of preventing or reducing ototoxicity in patients undergoing treatment with therapeutically effective amounts of aminoglycoside antibiotics are provided. The methods comprise administering an effective amount of an otoprotective agent comprising methionine or a methionine-like moiety to said patient prior to, simultaneously with, or subsequently to administration of the aminoglycoside antibiotic. Combinations of these time periods can also be employed.
US20110081348 Fungal signalling and metabolic enzymes Method of identifying an anti-fungal agent which targets as an essential protein or gene of a fungus comprising contacting a candidate substance with (i) a protein which comprises the sequence shown by SEQ ID NOS: 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, 48, 50, 53, 56, 59, 61 or 63, or (ii) a protein which has 60% identity with (i), or (iii) a protein comprising a fragment of (i) or (ii) which fragment has a length of at least 50 amino acids, or (iv) a polynucleotide that comprises a sequence which encodes (i), (ii) or (iii), or (v) a polynucleotide comprising a sequence which has at least 70% identity with the coding sequence of (iv), and determining whether the candidate substance binds or modulates (i), (ii), (iii), (iv), or (v), wherein binding or modulation of (i), (ii), (iii), (iv), or (v) indicates that the candidate substance is an anti-fungal agent.
CN103143018A Oral formulations containing metformin and alpha-glycosidase inhibitor, and preparation method thereof The present invention provides an oral formulation which contains a secondary wet granule produced by coating a primary wet granule with a mixed aqueous solution of an alpha-glycosidase inhibitor and hydroxypropyl cellulose, wherein said primary wet granule is produced by combining a mixed powder comprising metformin and hydroxypropyl cellulose with an aqueous solution of hydroxypropyl cellulose serving as a binding solution. In addition, the present invention provides a method for preparing an oral formulation, comprising the steps of: injecting the mixed powder of metformin and hydroxypropyl cellulose into a fluidized bed granulator, and spraying the aqueous solution of hydroxypropyl cellulose onto the mixed powder to produce a primary wet granule; and spraying the mixed aqueous solution of alpha-glycosidase inhibitor and hydroxypropyl cellulose onto the primary wet granule in the fluidized bed granulator to produce a secondary wet granule.
US7173037 Compounds for trearment of cardiovascular disorders and hypotensive agents The present invention relates to compounds which stimulate soluble guanylate cyclase, to the preparation thereof and to the use thereof as medicaments, in particular as medicaments for the treatment of cardiovascular disorders and/or sexual dysfunction.
US7265146 Administering small molecule compounds, especially acids or esters, that inhibit the interaction between alpha 4 integrins and ligands MAdCAM and/or VCAM for treatment of chronic inflammatory diseases such as arthritis, asthma, multiple sclerosis, Chrohn's disease, ulcerative colitis, and hepatitis C Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhibit binding of ligands for α4 integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with α4 integrins or their ligands.
CN1947794B Medicine composition containing sulfonylurea compounds and phenoxy acid type compounds A medical composition used for preparing the medicines for preventing and treating hyperglycemia, hyperlipemia and cerebrovascular and cardiovascular diseases caused by said hyperglycemia and/or hyperlipemia contains the glimepiride or its active metabolite or its derivative, phenyloxy acid type compounds or their active metabolits or salts or esters, and the pharmacologically acceptable carrier.
EP1896404A1 Pleuromutilin derivatives containing a hydroxyamino- or acyloxyaminocycloalkyl group The present invention relates to Compounds of general formula (I), wherein R is hydrogen and R1 is hydroxy or acyloxy, or R is acyl and R1 is hydroxy or acyloxy, X is sulphur, oxygen or NR10, wherein R10 is hydrogen or (C1-4)alkyl; Y is sulphur or oxygen; R2 is hydrogen or one or more substituents, e.g. including substituents such as conventional in organic, e.g. (pleuro)mutilin, chemistry; R4 is hydrogen or (C1-4)alkyl; R5 is hydrogen or (C1-4)alkyl; R3 and R3' are hydrogen, deuterium, or halogen; R6, R7 and R8 are hydrogen, halogen or deuterium; m is a number selected from 0 to 4, n is a number selected from 0 to 10, and p is a number selected from 0 to 10; with the proviso that n plus p are at least 1. These Compounds are usefül as pharmaceuticals, particularly as antimicrobials.
US20100087433 Methods of inhibiting tryptophan hydroxylase Compounds, compositions and methods of treating serotonin-mediated diseases and disorders are disclosed.
WO2012013117A1 Pharmaceutical composition of temozolomide comprising vitamin c or vitamin c derivative and preparation method thereof The present invention provides a pharmaceutical composition of temozolomide and a preparation method thereof. The composition comprises temozolomide or a pharmaceutically acceptable salt thereof, vitamin C, and a vitamin C derivative. The vitamin C and the vitamin C derivative allow the stability of temozolomide to be ensured, and the solubility thereof to be improved. The safety and effectiveness of using the medicament is thus effectively improved.
CN103127005A Preparation method of novel dopamine brain-targeting nano-particles The invention discloses a preparation method of novel dopamine brain-targeting nano-particles. According to the method, a certain concentration of a polyvinyl alcohol water solution is prepared, and is subjected to standing overnight; the solution is cooled, and Tween-60 is added; a polyer/dichloromethane solution is prepared; the solution is completely dissolved, and polyvinyl pyrrolidone and Span-60 are dissolved into the dichloromethane solution; the mixture is stirred until sufficiently dissolved, such that an oil phase is obtained; dopa with different ratios are dissolved, such that an internal water phase is obtained; under magnetic stirring, the internal water phase is slowly added into the oil phase by using a barrel syringe; stirring and emulsification are continued under the speed; the oil phase is transferred into an outer water phase by using a pipette gun; the temperature is increased, such that dichloromethane is evaporated; the product is washed multiple times by using double-distilled water, and is filtered and lyophilized until constant weight is achieved, such that DA-packaging polymer microspheres are obtained. The novel degradable biological nano-grade material provided by the invention has relatively high bioavailability. The preparation method has the advantages of simple method, low cost, and high stability.
US8273349 Binding member which binds to both lewis-Y and lewis-B haptens, and its use for treating cancer The invention relates to the use of a binding member which binds to LewisY and Lewisb haptens in the treatment of tumours and leukaemia. The binding member may be an antibody which binds to LewisY and Lewisb haptens and cancer cells and induces cells death.
WO2007053093A1 Chroman compounds as 5 ht1b antagonists Compounds according to Formula (I) wherein X and R are as defined in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
EP1545531A1 Use of 5-ht2 receptor antagonists for the treatment of sleep disorders The invention relates to the use of 5-HT2 receptor antagonists for producing a medicament which extends non-REM sleep and REM sleep.
US20080069903 Electrical producing creams New electrical producing creams are provided. In one embodiment, the electrical producing creams comprise menthol and camphor, preferably provided as part of a base gel, supplemented with potassium and a source of oxygen. The most preferred base gel is sold under the name SOMBRA. In another embodiment, the electrical producing creams comprise potassium and a source of oxygen supplemented with optional active and inactive ingredients. The most preferred source of oxygen is a chlorite (e.g., sodium chlorite) and/or spirulina. The electrical producing creams provide high metabolic activities and sustain those activities over prolonged periods of time, thus being useful for treating a large variety of ailments, including diabetic neuropathy, post hepatic neuralgia, scleroderma, psoriasis, strain, spasticity, headaches, neuropathy secondary to drugs, peripheral neuropathy, leg pain, muscle cramps, muscle aches and pains, bruise, sinusitis, sprain, arthritis, joint pain (arthralgia), and edema.
CN103550221A Compound injection containing tiamulin fumarate and cefquinome sulfate The invention relates to preparation for applying sucrose acetate isobutyrate (SAIB) to veterinary oil injections and particularly relates to preparation for applying a combination of SAIB and hydrogenated castor oil or a combination of SAIB and aluminum stearate to a compound long-acting injection containing tiamulin fumarate and cefquinome sulfate, wherein a dispersion medium is one or a mixture of more than one of isopropyl myristate, benzyl benzoate and ethyl oleate. The injection has the advantages of good slow-release effect, stable property, good histocompatibility and easiness in preparation.
US20100240747 Motuporamine Mimic Agents Disclosed herein are motuporamine mimic agents and methods of making and using same. Particularly exemplified are motuporamine mimic agents comprising cytotoxic activity and/or anti-metaplastic activity.
CN1748691A Albendazole jelly for treating adenoid hypertrophy The present invention relates to the preparation process of nasal albendazole jelly and the application of the nasal albendazole jelly in treating adenoid hypertrophy.
CN102198199B Plaster for treating facial nerve paralysis The invention relates to a plaster for treating facial nerve paralysis and a preparation method thereof. The plaster is characterized by comprising the following materials, by weight, 3-5 parts of centipede, 5-15 parts of pangolin, 5-25 parts of whole worm, 15-26 parts of white batryticated silkworm, 5-15 parts of rhizoma typhoon, 5-15 parts of radix cyathulae, 10-20 parts of safflower, 5-8 partsof ground beetle, 5-15 parts of catnip, 5-15 parts of divaricate saposhnikovia root, 10 parts of monkshood, 10 parts of aconitum kusnezoffii, 5-10 parts of rhynohophylla, 5-15 parts of pawpaw, 3-6 parts of licorice, 5-10 parts of herba siegesbeckiae, 11-15 parts of cassia twig, 5-15 parts of myrrh, 5-15 parts of frankincense, 150-180 parts of yellow lead and 800-1000 parts of scent oil. The invention is aimed to provide a facial nerve paralysis treating medicament, which has a low price, short treatment course, no toxic or side effect, no pain and a good curative effect.
US20130095155 Topical vitamin d and ubiquinol oral supplement compositions A topical vitamin D and UBIQUINOL supplement composition useful in treating oral inflammation and reducing oxidative stress comprising: a supplement mixture of vitamin D and UBIQUINOL in an aqueous-free emulsion containing: spilanthes extract, stabilizing compositions for UBIQUINOL and trans-oral mucosal absorption facilitators for the supplement mixture; where the emulsion forms a mucoadhesive gel in the presence of saliva, that effects passive diffusion through the oral mucosa of the supplement mixture and spilanthes extract regulating: in vivo availability and immune response of the supplement mixture, and maintaining adequate levels of circulating vitamin D and of adjunctively administered UBIQUINOL, while minimizing the risk of hypercalcemia.
US20090035274 Treatment and/or prevention of cancer and/or arthritis The invention relates to the use of INSP163 for treatment and/or prevention of cancer and/or musculoskeletal/connective tissue disorder, in particular of lung cancer and/or osteoarthritis. Combinations of INSP163 with an interferon, a TNF antagonist or a further anti-cancer or anti-arthritis agent are also within the present invention.
US20110257109 Use of drugs that activate p2y receptors to enhance synaptogenesis The present invention encompasses compositions and methods that activate P2Y receptors for the increased production of new synapses in the central nervous system. The formulations of the invention may be administered to a healthy subject or to a subject in need thereof to restore synapses.
EP2149575A1 Diazabicyclic compounds as opioid receptor agonists Nonane and decane diazabicyclic derivatives having homopiperazine as main ring, having affinity for the opioidergic µ and/or δ and/or k receptors and/or for all their receptorial subclasses, with central and/or peripheral activity, having formula (I), the isomeric forms and their mixtures included, wherein one or more atoms are in the corresponding isotopic forms: wherein: - n is an integer equal to 1 or 2; - one of the substituents R and R1 of the nitrogen atoms of the diazabicyclic ring is a -C(O)-RB group, wherein RB is a C1-C10 alkyl group, linear or branched when possible, - the other remained substituent of R and R1 has the meanings reported in the description.
US7078386 Enhancing agent for nerve growth factor production comprising a compound having a coumarin backbone or a compound having a 2-dimethyl chroman backbone The present invention relates to a medicament, a food, a beverage or a feed, each comprising as an effective ingredient a compound having an enhancing action for NGF production, which is effective for a treatment, an amelioration of symptom, prevention or the like of a disease requiring enhancement of NGF production, wherein the compound has a coumarin and/or chroman backbone. Since no toxicity is especially found in the effective ingredient of the present invention, and there is no risk of incidence of adverse actions, the treatment or the like of the above disease can be safely and appropriately carried out.
CN102772396A Cooperatively used combination type preparation for cleaning and sterilizing skin after being bitten or scratched by animals The invention relates to a cooperatively used combination type preparation for cleaning and sterilizing skin after being bitten or scratched by animals. The purpose of the invention is to provide a cooperatively used combination type preparation for cleaning and sterilizing skin after being bitten or scratched by animals with the characteristics of simple preparation, good stability, ease use and good use effect. The technical solution provided by the invention is as follows: the cooperatively used combination type preparation for cleaning and sterilizing skin after being bitten or scratched by animals is characterized in that the combination type preparation comprises a weakly alkaline cleaner and a skin antibacterial spray; the raw materials of the weakly alkaline cleaner include benzalkonium chloride or benzalkonium bromide, 30% dodecyl dimethyl amine oxide solution and polysorbate 20; the raw materials of the skin antibacterial spray include benzalkonium bromide, or benzalkonium chloride, or chlorhexidine, or chlorhexidine acetate, or chlorhexidine hydrochloride, or chlorhexidine citrate, or 20% chlorhexidine gluconate solution and polysorbate 20. The preparation provided by the invention is applied to the treatments of cleaning and sterilizing the skin wounds after being bitten or scratched by dogs, cats and other animals.
CN102625807A 4-substituted pyridin-3-yl-carboxamide compounds and methods of use The invention relates to compounds of Formula (I) which are useful as kinase inhibitors, more specifically useful as PIM kinase inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same, either alone or in combination, to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
DE102004056838A1 Composition containing a sympathomimetic, useful for treating pruritus ani and hemorrhoids, optionally also containing a coumarin and local anesthetic Formulation (A) containing at least one sympathomimetic (I). - ACTIVITY : Antipruritic; Vasotropic. Patients with hemorrhoids of stages I or II were treated with anal inserts, of cotton-viscose blend, impregnated with 0.1% xylometazolin. 21 of 23 subjects were free of discomfort after 24 hours, and all were free after 36 hours. - MECHANISM OF ACTION : (I) has a vasodilating action that facilitates drawing back of hemorrhoids into the anal passage and it inhibits coagulation of blood in hemorrhoids.
CN1732908A Borneol contained spray The invention provides a borneol contained spray wherein the medicinal solution contains 0.01-20 wt% of borneo camphor, 5-40 wt% of ethanol, natural or synthesized neutral fatty oil, asarum oil, sandalwood oil, galange oil, long pepper oil and other pharmacological active components.
US7138148 Use of extracts of Ginkgo biloba for preparing a medicament intended to treat sarcopenia The invention concerns the use of Ginkgo biloba extracts, and in particular Ginkgo biloba extracts comprising 20 to 30% of flavoneglycosides, 2.5 to 4.5% in total of gingkolides A, B, C and J, 2 to 4% of bilobalide, less than 10% of proanthocyanidins and at least 10 ppm of alkylphenol type compounds, for preparing a medicine for treating sarcopenia.
WO2010029562A1 Bioactive composition for the treatment of the hiv/aids, method for manufacturing and using the same The present invention is about a bioactive composition for the treatment of HIV, particularly by the removal of the most prominent HIV antigen glycoproteins. The present invention further related to the method for making and using such composition.
CN101274039A Tea pigment sustained-release dropping pills and method of preparing the same The invention relates to a pharmaceutical composition which has the functions of refreshing mind, resolving phlegm and eliminating fat and is applied to treating dizzying, chest distress, chest pain, hyperlipidemia, coronary heart disease, angina, cerebral infarction and other similar symptoms caused by intermingled phlegm and blood stasis. The pharmaceutical composition of the invention aims at compensating for the shortage of tea pigment oral preparations and providing an oral preparation tea pigment sustained-release dropping pill of the pharmaceutical composition which can make effect quickly, has high bioavailability, long effective time, few medicine taking times, less toxicity and side effects, high drug contents, little and accurate dose, convenient use, low cost and easy carrying.
WO2014127315A1 Centrally active and orally bioavailable antidotes for organophosphate exposure and methods for making and using them In alternative embodiments, the invention provides nucleophilic hydroxyimino- acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nerve system (CNS). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino- acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps. In alternative embodiments, the invention provides pumps, devices, subcutaneous infusion devices, continuous subcutaneous infusion devices, infusion pens, needles, reservoirs, ampoules, a vial, a syringe, a cartridge, a disposable pen or jet injector, a prefilled pen or a syringe or a cartridge, a cartridge or a disposable pen or jet injector, a two chambered or multi- chambered pump, a syringe, a cartridge or a pen or a jet injector, comprising a compound of the invention.
WO2014060941A3 Compounds and compositions of neuroprotective agents for treatment of neurological and neurodegenerative diseases Disclosed are compounds of formula I, their pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I) are also disclosed. Such compositions may be used for treating seizures, Huntington's disease, spasms, mental disease, mental disorders, schizophrenia, depression, stress, bipolar disorder, Alzheimer' s diseases, anxiety, ADHD, dementia, mood disorders, PTSD, sleeplessness, epilepsy, migraine, psychosis, OCD, autism, anxiety disorders, dementia, mania and cognitive disorders.
CN102133196A Potassium ion binding polymers for pharmaceutical compositions The invention provides pharmaceutical compositions comprising potassium binding polymers. The potassium binding polymer is a crosslinked cation exchange polymer, and comprises a cationic counter-ion to potassium and acid groups, wherein the acid groups are selected from carboxylic groups and phosphonic groups. The fraction of ionization of the acid groups is greater than about 75% at the physiological pH in the colon. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hyperkalemia, such as hyperkalemia caused by renal failure and/or the use of hyperkalemia causing drugs.
WO2006091010A1 Composition comprising coenzyme q10 as effective ingredient Disclosed is a pharmaceutical composition for eliminating and alleviating alcohol -related disorders. The pharmaceutical composition for eliminating and alleviating alcohol -related disorders including hangover symptoms or flushing comprises coenzyme Q10, which removes reactive oxygen species considered to be a cause of hangovers, as an effective ingredient. Also disclosed is a treatment method of alleviating alcohol-related disorders by taking the pharmaceutical composition before, during, after, or the day after alcohol consumption. Further disclosed is a functional food supplemented with the pharmaceutical composition, the food being taken as a side dish. The practical use of the pharmaceutical composition may greatly reduce the social side effects of alcohol consumption.
CN101301272A Sustained-release agent containing mezlocillin and uses thereof The invention discloses a sustained release injection containing mezlocillin, which consists of sustained release microspheres and menstruum, wherein, the sustained release microspheres contain sustained release excipient and penicillin antibiotics, the menstruum is special menstruum containing suspending agents such as sodium carboxymethyl cellulose and so on, and the viscosity is between 100 and 3000cp (at the temperature of between 20 and 30 DEG C); the sustained release excipient is selected from EVAc, polifeprosan, PLA, PLGA, decanedioic acid copolymers, albumin glue, gelatin and so on; and the sustained release microspheres can also be prepared into sustained release implant. The sustained release implant and the sustained release injection are locally placed or injected on a bacteria focus, which can slowly release medicine at a local lesion for 5 to 30 days and apparently decrease the systemic toxicity of the medicine when the effective medicine concentration of the local lesion is effectively obtained and maintained. The sustained release injection has a remarkable and unique treatment effect on infections caused by staphylococcus, streptococcus, peptostreptococcus, acne propionate bacillus, enterobacter, tubercle bacillus, gonococcus or meningococcus and so on, particularly on local lesions such as chronic osteomyelitis, severe bedsore, refractory skin ulcer, diabetic foot and femoral head necrosis of diabetes, and various abscesses and so on.
WO2009071731A1 Use of an ionic complex of gentamicin : aot for the treatment of brucellosis The invention relates to an ionic complex of gentamicin and sodium bis(2-ethylhexyl) sulfosuccinate (AOT) in a molar ratio of 1:5 (gentamicin : AOT) for the production of a drug intended for the treatment of a disease caused by a bacterium of the genus Brucella. In one embodiment of the invention, the therapeutic ionic complex is also treated by: (a) dissolving the gentamicin : AOT ionic complex in an organic solvent; (b) spraying the solution resulting from step (a) into a compressed fluid miscible with the organic solvent, which acts as an antisolvent and causes the precipitation of a solid; and (c) separating the solid resulting from step (b).
EP1908477A2 Combination of temozolomide and pegylated interferon-alpha for treating cancer A method for treating a human patient afflicted with cancer, comprising administering therapeutically effective amounts of temozolomide and pegylated interferon alpha to such a patient.
EP1177185B1 4, 5, 6, 7-tetrahydroindazole derivatives as antitumor agents Compounds which are 4,5,6,7-tetrahydroindazole derivative formula (I), wherein the dotted line (x) represents a single or double bond; n is 0 or 1; R1, R2 and R3 have the meanings reported in the description; Ra, R'a, Rb, R'b, Rc, R'c have the meanings reported in the description, also comprising that Ra and Rb together and/or Ra and Rc together form a N-alkyl-piperydinyl ring with 1 to 6 carbon atoms in the alkyl chain or a phenyl ring; or pharmaceutically acceptable salts thereof, are useful for treating cell proliferative disorders and Alzheimer's disease.
US7226758 glial derived neurotrophic factor (GDNF) isolated from serum-free growth conditioned medium of glioblastoma cells; for preventing and treating nerve damage and nerve related diseases such as Parkinson's disease; genetic engineering A novel neurotrophic factor referred to as glial cell line-derived neurotrophic factor (GDNF) has been identified and isolated from serum free growth conditioned medium of B49 glioblastoma cells. Rat and human genes encoding GDNF have been cloned and sequenced. A gene encoding GDNF has been subcloned into a vector, and the vector has been used to transform a host cell in order to produce biologically active GDNF in a recombinant DNA process.
CN1840179A Application of bovine lactoferricin in preparation of medicine for treating HP infected gastric disease The invention relates to the use of Bovine Lactoferrin in preparing medicaments for the treatment of gastritis and gastric ulcer infected by Helicobacter Pylori, wherein the constituents of the medicaments include Bovine Lactoferrin 100-250mg, Rabeprazole 10-20mg, Clarithromycin 300-500, tinidazole 300-500mg.
WO2011111581A1 Therapeutic agent and therapeutic device for alleviating ischemia-reperfusion injury Disclosed is a therapy for alleviating ischemia-reperfusion injury, which has few adverse side effects and can inhibit the invasion of neutrophils and the activation of platelets during ischemia reperfusion. The therapy comprises administering a mixed gas through inhalation to a patient who is intended to receive reperfusion, for a period between a time point that is immediately prior to the initiation of the ischemia-reperfusion and a time point that is shortly after the initiation of the reperfusion, wherein the mixed gas comprises 21 to 98% of oxygen, 0.1 to 4% of hydrogen and 40 to 80 ppm of nitrogen monoxide, with the remainder being an inert gas such as a nitrogen gas and a helium gas.
US20080027061 omega-Carboxy Aryl Substituted Diphenyl Ureas As p38 Kinase Inhibitors This invention relates to the use of a group of aryl ureas in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.
US20080131494 Dermal Penetration enhancers and drug delivery systems involving same The invention relates to a method for treatment or prophylaxis of a disease or condition in an animal comprising administering to a mucosal membrane of said animal in need of such treatment a therapeutically effective amount of a drug delivery system comprising at least one physiologically active agent or prodrug thereof and at least one penetration enhancer selected from safe ester sunscreens.
WO2012021409A2 Anthraquinone Analogs Anthraquinone analogs, methods for synthesizing anthraquinone analogs, and methods for inhibiting growth of one or more types of cells using anthraquinone analogs. Anthraquinone analogs can be synsthesized according to methods described herein. Optionally, the synthesis methods described herein include choosing an appropriate leaving group for selectively producing 1-alkyl-1H-naphtho[2,3-d]triazole-4,9-diones or 2-alkyl-2H-naphtho[2,3-d]triazole-4,9-diones. Anthraquinone analogs can include various functional groups that affect their ability to inhibit the growth of various cell types. For example, some anthraquinone analogs disclosed herein have antimicrobial activity while seemingly similar compounds demonstrate anticancer activity but lesser antimicrobial activity.
EP1438377B1 Cholesterol lowering structured lipids with omega 3 pufa Unique structured lipids obtained from interestifying coconut oil with free fatty acids obtained from hydrolysis of triglycerides of an animal source, said structured lipids rich in omega-3-poly unsaturated fatty acid and medium chain fatty acid and a process for the production of said structured lipids.
US20090053763 Tumor endothelial marker 7-alpha molecules and uses thereof The present invention provides Tumor Endothelial Marker 7α (TEM7α) polypeptides and nucleic acid molecules encoding the same. The invention also provides selective binding agents, vectors, host cells, and methods for producing TEM7α polypeptides. The invention further provides pharmaceutical compositions and methods for the diagnosis, treatment, amelioration, and/or prevention of diseases, disorders, and conditions associated with TEM7α polypeptides.
CN101077344A Infusion preparation of ibuprofen and preparation method thereof The present invention provides one kind of brufen transfusion preparation and its preparation process, and features that the brufen transfusion preparation is prepared with brufen as main component, glucose or sodium chloride, alkaline cosolvent, propylene glycol or alcohol, sodium bisulphate, EDTA-2Na and water for injection, and through a certain technological process. The brufen transfusion preparation is superior to common orally taken brufen preparation and injection, and has short production period, high bioavailability, fast acting and other advantages.
US7375109 Glycine-substituted thieno[2,3-d]pyrimidines with combined LH and FSH agonistic activity The present invention resides in glycine substituted thieno[2,3-d]pyrimidine derivatives according to general formula I, or a pharmaceutically acceptable salt thereof, wherein X is O or H,H A is S, NH, N(R6), O or a bond; R1 is (1-4C)alkyl, (2-4C)alkenyl, phenyl or (2-5C)heteroaryl, the phenyl or heteroaryl ring optionally being substituted with one or more of the group of substituents: hydroxy, halogen, nitro, trifluoromethyl, cyano, amino or (1-4C)(di)alkylamino and R2 is H, (1-4C)alkyl, (1-4C)alkoxy(2-4C)alkyl or hydroxy(2-4C)alkyl; R3 and R4 can be independently selected from H and hydroxy(1-4C)alkyl; R5 is H or (1-4C)alkyl; R6 can be selected from the same groups as described for R1. The compounds of the invention have LH as well as FSH receptor activating activity and can be used in fertility regulating therapies.
CN103520181A Application of phyllanthoid A in preparing medicament for preventing and treating renal fibrosis The invention provides an application of phyllanthoid A in preparing a medicament for preventing or treating renal fibrosis and belongs to the technical field of novel applications of medicaments. The application of the phyllanthoid A in preparing the medicament for preventing or treating renal fibrosis is published for the first time. As a skeleton type of the phyllanthoid A belongs to a brand-new skeleton type, the phyllanthoid A has strong activities for inhibiting renal fibrosis and remarkable substantial characteristics and has significant progresses apparently when being used for preventing and treating renal fibrosis at the same time.
EP2744483A1 Delivery system for specifically targeting cancer cells and method of use thereof Methods for prevention, treatment or inhibition of the growth or metastasis of cancer cells in a subject are disclosed. One method comprises the step of administering to the subject a therapeutically effective amount of tumor associated antigen binding ligand-coated planetary ball milled (PBM) nanoparticles containing a cytotoxic agent.
CN102247546A Prescription for relieving exterior syndrome and dispelling heat The invention aims to provide a prescription for relieving exterior syndrome and dispelling heat. The formula of the prescription comprises 20 grams of honeysuckle, 6 grams of mint, 20 grams of gypsum, 15 grams of anemarrhena asphodeloides, 20 grams of astragalus, 20 grams of reed rhizome, 5 grams of liquoric root and 10 grams of fineleaf schizonepeta herb. A dose is taken each day at two times.
CN1836667B Eye drop There obtain an eye drop that further enhances intraocular pressure lowering effect than a single use of a nitric oxide donative compound and treats glaucoma, ocular hypertension, etc., without using a multiple drug. The eye drop comprises a nitric oxide donative compound and alginic acid or its salt. The method for enhancing the efficacy of a nitric oxide donative compound comprises adding alginic acid or its salt to the eye drop comprising a nitric oxide donative compound as an active ingredient. The efficacy enhancer of a nitric oxide donative compound comprises alginic acid or its salt asan active ingredient.
CN101843636B Preparation process of non-PVC-soft-bag-packaged hemofiltration replacement liquid and product The invention provides a preparation process of non-PVC-soft-bag-packaged hemofiltration replacement liquid and a product. The preparation process is characterized by comprising the following steps: a. preparing medicine liquid: adding water for injection into a tank for high-concentration preparation, and then adding anhydrous glucose, and stirring to be dissolved; then adding 0.05% (W / V) of activated carbon, and holding at a temperature of 40 DEG C-70 DEG C, stirring and de-carbonizing for 30 minutes; removing carbon through titanium rod filtration, taking clear liquid to be put in a tankfor dilution preparation, and adding the water for injection to the full amount, and evenly stirring; b. filling: filtering through a filter, bag-making and filling in a non-PVC soft plastic infusionbag with a double-pipe and double-valve structure, adding a stopper and sealing, wherein the reserving space of the soft infusion bag is 15% or above 200ml; c. sterilizing; and d. packaging. Enough liquid adding space is reserved, the double-pipe and double-valve structure can facilitate to add liquid so as to prevent the secondary pollution and facilitate the clinical flexible adjustment of prescriptions; and the non-PVC soft infusion bag does not contain plasticizers, adhesives and other substances harmful to the human body, and does not introduce new harmful substances.
CN102844324A Methods for producing amino-substituted glycolipid compounds The invention describes a method of preparing a compound of formula (I): wherein: a first group selected from R1, R2 and R3 is an amino- or N-acylamino monosaccharide moiety, the acyl group having 1 to 6 carbon atoms, or an oligosaccharide chain comprising 2 to 4 monosaccharide moieties, at least one of which is an amino- or N-acylamino monosaccharide moiety; a second group selected from R1, R2 and R3 is a saturated or unsaturated acyi group having 3 to 40 carbon atoms; and a third group selected from R1, R2 and R3 is hydrogen, the method comprising contacting a monoacylglycerol, the acyl moiety thereof being a saturated or unsaturated acyl group having 3 to 40 carbon atoms, or an activated derivative thereof, with a source of amino- or N-acylamino monosaccharide moiety, or an activated derivative thereof, and, if required, a source of unsubstituted monosaccharide moiety, or an activated derivative thereof, optionally in the presence of a suitable catalyst or activating agent. Novel compounds, as well as In situ methods for producing the compounds, and their use as emulsifiers, surfactants and antimicrobial agents, particularly in foodstuffs and detergent compositions, are also described.
WO2008148269A1 Anti-tumor medicine containing betulinic acid derivatives The present application provides an anti-tumor medicine with betulinic acid derivatives 3-deoxy-3-oxo-dihydrobetulinic acid or 3-deoxy-3-oxo-betulinic acid as the active ingredient. The said betulinic acid derivatives have the effect of inhibiting thirty-one kinds of tumor cell lines in the cytotoxicity test, especially human prostatic cancer cell LnCAP, human lung cancer cell NCI-H23, human colon cancer cell HCT-116, human melanoma cell G-361, human glioblastoma cell U-251.
EP1675833A1 1h-imidazole derivatives as cannabinoid receptor modulators The invention relates to a group of 1H -imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders in which cannabinoid receptors are involved. The compounds have the general formula (I) wherein R, R1-R4 and X have the meanings given in the specification.
WO2009059961A3 A method of hormone suppression in humans The present invention relates to a glycine transporter-1 inhibitor having the formula (I) wherein X is 1-3 substituents selected from H, halogen, methyl, methoxy, trifluoromethyl and trifluoromethoxy and Y is 1-3 substituents selected from H, methyl and halogen or a pharmaceutically acceptable salt thereof for use in a treatment in humans to suppress the level of one or more hormone selected from luteinizing hormone, follicle-stimulating hormone, estradiol and testosterone. The present invention further relates to such a glycine transporter-1 inhibitor as part of a contraceptive regimen or as a treatment for hypersexuality.
EP2332545A1 Composition for treating central nervous system disorders The present invention provides a method and composition for treating a central nervous system disorder in a mammalian subject, which comprises administering an effective amount of a 11-deoxy-prostaglandin compound to a subject in need thereof. The invention also provide novel 11-deoxy-prostaglandin compound.
CN103703000A Fused tricyclic dual inhibitors of CDK 4/6 and FLT3 Compounds of Formula (I) are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula (I) have the following structure: where R1 is a group of Formula (IA), Formula (IB), Formula (IC), or Formula (ID) and the definitions of the other variables are provided herein.
US20120094971 Compositions Including 6-Aminohexanoic Acid Derivatives As HDAC Inhibitors This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.
US20090093512 1, 2, 3, 3a, 8, 8a-hexahydro-2, 7a-diada-cyclopenta[a]inden-7-one derivatives which bind to neuronal nicotinic acetylcholine specific receptor sites and are useful in modulating cholinergic function and in the treatment of addictive disorders The present invention relates to novel fused bicyclicpyrrolidine pyridone compounds of the formula (I) wherein R, RP and n are as defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions and their use in treating addictive disorders such as the use of tobacco or other nicotine containing products and in the treatment of neurological and mental disorders related to a decrease in cholinergic function.
CN101402543A Beta-elemi alkene bulk medicament and method of preparing its preparations The invention provides a method for preparing high-purity beta elemene from natural plants containing the beta elemene such as curcuma zedoary (earthnuts or tubers of the curcuma zedoary), cedronella (fresh leaves of the cedronella), yellowtop (roots, stems, leaves, flowers and seeds of the yellowtop) and so on, which can improve the production efficiency from starting materials to the high-purity beta elemene and reduce production cost. Compared with the prior art, the method is mainly different in that the roots, stems, leaves, flowers and seeds of the natural plants are taken as raw materials; oleum volatile of specific parts of the natural plants is obtained by methods for extracting different oleum volatiles, and is distilled by molecular distillation method to remove compositions with high boiling points and non-volatile compositions; impurity compositions are removed by the ethanol extraction method and silver nitrate complex extraction method; and finally the beta elemene with the content between 95.0 and 99.9 percent is obtained through reduced pressure distillation or rectification. The bulk pharmaceutical chemicals not only can be prepared into oral dosing preparation such as emulsion oral liquid, self-emulsifying/ self-microemulsifying capsules, soft capsules and so on, but also can be prepared into non-alimentary dosing preparation such as emulsion injection, liquid drugs injection, transdermal absorbent, lung sprays, suppository and so on. The method has the advantages of novel design, concise operating steps, mild operating conditions and improvement of the production efficiency of the beta elemene.
CN102924556A (20S, 24R)-ocotillol type ginsenoside derivative having antibacterial activity and preparation method and application thereof The invention relates to the fields of organic synthesis and pharmaceutical chemistry, in particular to a (20S, 24R)-ocotillol type ginsenoside derivative having represented in a structural formula (I). The invention further discloses a reparation method of the (20S, 24R)-ocotillol type ginsenoside derivative, pharmaceutical compositions containing the derivative and anti-bacterial and anti-infection application.
US7476670 anticancer/antiproliferative activity; antifungal agents; protein kinases inhibitors in perticular Focal Adhesion Kinase inhibitors and fungal CIV1 protein kinase inhibitors; N-[6-(5,6-dichloro-2,3-dihydro-1H-indol-1-yl)-9H-purin-2-yl]-1,4-cyclohexanediamine dihydrochloride The invention relates to novel products of formula (I): in which: Y represents N, O, S, CHR3 or ═CR3 the dashed line representing a single or double bond, R and R1 represent in particular H, Hal, OH, alkyl, alkoxy, cyano, NO2, NR4R5, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, —S(O)n-NR4R5 with n representing 0 to 2, acyl, —NH—CO-alkyl or —NH—CO—NH-phenyl, R3 represents H, Hal, alkyl, cyano, NO2, NR4R5, trifluoromethyl or aryl, R2 represents R4, OR4, SR4 or NR4R5, R4 represents H, alkyl, cycloalkyl or aryl, either R4 and R5 are chosen from the values for R4, or R4 and R5 form, with N, a heterocyclic radical which may contain N, O and S, all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products.
US7390805 Tyrosine kinase inhibitors; antiproliferative agents; antitumor agents The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.
EP2004619A1 1-phenylsulfonyl-diaza heterocyclic amide compounds and their uses as modulators of hydroxsteroid dehydrogenases Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: (I) where R5,R6,R7,R8,R9,R10, m, Q, X, and Y are set forth in the description.
US20110047631 Heat shock protein deficiencies as model systems for brain pathology and cancer The invention provides non-human transgenic animals as models of neurodegenerative brain pathology, including, but not limited to, Alzheimer's disease (AD), and cancer. The non-human transgenic animals of the present invention include an exogenous DNA that reduces or eliminates the expression and/or function of a molecular chaperone, including, but not limited to heat shock protein 110 (Hsp1 10) or heat shock protein 70 (Hsp70). These non-human transgenic animals may be used in methods of screening and identifying compounds useful for the prevention and/or treatment of neurodegenerative brain pathology and/or cancer.
US20050019376 Containing at least one active ingredient and a confectionery composition such as fat, amorphous sugar glass, or fondant; polarized light transmission; especially for pediatric and geriatric applications A dosage form comprises an active ingredient and a confectionery composition. In one embodiment the relative standard deviation of the weight of the dosage form is less than 1%, and the dosage form has at least one face. In another embodiment, a dosage form comprising an active ingredient and a confectionery composition wherein the dosage form has at least one face, does not have a free formed surface, and has a mean polarized light transmission at the angle of maximum extinction which is not greater than the mean polarized light transmission of the dosage form at the angle of maximum transmission. The active ingredient may be a pharmaceutically active agent.
CA2562526A1 Selected cgrp antagonists, method for producing the same and the use thereof as drugs The invention relates to the CGRP antagonists of general formula (I), wherein A, X and R1 to R3 are defined as in claim 1. The invention also relates to the tautomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof and to the hydrates of said salts, especially their physiologically acceptable salts with inorganic or organic acids, to drugs comprising said compounds, to their use and to a method for producing the same.
CN1799552A Single sialic acid tetrahexose ganglioside preparation method The invention relates to a method for preparing mono sialic acid hexose ganglioside sodium agent, comprising removing integument and blood vessel from the fresh or frozen pig brain or cattle brain, pushing for dewatering with cold acetone for several times, filtering with organic membrane, pouring out the acetone, and treating into acetone powder, packing, and conserving; extracting clarified solution from acetone powder, filtering with ultra-filter membrane and getting ultra-filtrate, extracting with tobacco extract, sodium filtering with sodium filter membrane to remove small molecule, abandoning the filtrate, getting clean condensed liquid of the mono sialic acid hexose ganglioside sodium agent; sterilizing and getting the refine product. The invention changes the polarity of the extracting organic solvent, which makes the ganglioside be released almost fully into the solution. The invention employs the ionic sodium filter membrane to separate and converse the ganglioside depending on the its number difference in sialic acid and carboxyl groups, and employs modern membrane separation technique to replace filling material and column suction technique, which saves large quantity of solvent and time, and increases productivity.
CN101906056A Cycloalkane amine compound as M2 inhibitor and application thereof The invention discloses a cycloalkane amine compound of a general formula I or II, or pharmaceutically acceptable salt thereof, or substituted group defined in the description; the cycloalkane amine compound of the general formula I or II, or pharmaceutically acceptable salt can be used for preparing medicine for preventing and treating flue; as the M2 ion channel protein inhibitor, the compound can stop copy of the flue virus, and treat influenza, specifically the influenza A.
US7019000 administering nitrogen-sulfur compounds, e.g. 4,4-dithiodimorpholine to inhibit binding of the E6 protein by human papilloma virus; treatment of cervical cancer The invention provides agents and compounds (see (I) and (II)) for use in the treatment or prophylaxis of disease conditions caused or exacerbated by mammalian papillomaviruses, such as human papillomaviruses, as well as methods for the treatment or prevention thereof. In said formulae, R1–R4 and n are as defined herein.
CN1965943A Drink for relieving foul breath Disclosed is a beverage for treating foul breath which is prepared from raw materials of mung bean, mentha, clove, musk melon seeds, brown sugar, gypsum, wrinkled giant-hyssop, ledebouriella root, cape jasmine and licorice root through baking treatment and pure water dilution.
EP2552907A1 Pyridyltriazoles The present invention encompasses compounds of general formula (1) wherein the groups R0 to R3 and L are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
WO2006041961A1 Arylthioindole tubulin polymerization inhibitors and methods of treating or preventing cancer using same The present invention features arylthioindole compounds, pharmaceutical compositions of arylthioindole compounds and methods of treating a patient suffering from cancer or inflammatory, cardiac, or helminthic diseases, the method comprising administering to a patient one or more arylthioindole compounds of the invention.
WO2008020042A1 Use of 2, 5-dihydroxybenzene derivatives for the treatment of tissue reactive diseases The present invention relates to the use of a compound of Formula (I') or pharmaceutically acceptable salt or solvate, isomer or prodrug thereof in the manufacturing of a medicament for the treatment and/or prophylaxis of any of the diseases selected from the group consisting of benign prostatic hyperplasia, Barrett's disease, asthma, skeletal muscle and tendon repair, Crohn's disease, ulcerative colitis and leishmaniasis.
WO2012003562A4 Antineoplastic pharmaceutical compositions containing substituted nitroimidazoles The present invention describes antineoplastic pharmaceutical compositions containing substituted nitroimidazole. These compositions may be used for treating early-stage neoplasias or in combination with drugs with antitumour action already established for more advanced stages of the disease.
US7368571 HIV-Integrase inhibitors, pharmaceutical compositions and methods for their use Bicycling hydroxamate compounds represented by the Formula I: are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.
EP2662367A1 Novel indole or indazole derivative or salt thereof The the present invention relates to provision of a novel indazole compound which is capable of inhibiting HSP90 and shows a cytostatic effect on cancer cells. The present invention also relates to provision of a drug useful for preventing and/or treating, on the basis of an HSP90 inhibitory effect, a disease in which HSP90 participates, in particular, cancer. A compound represented by the general formula (I) or a salt thereof: wherein X represents CH or N; any one or two of Y1, Y2, Y3, and Y4 represent C-R3 or N, and the others represent CH; A and B are the same or different and represent an optionally substituted monocyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R1 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R2 represents a hydrogen atom, a halogen atom etc.; R3 represents a hydrogen atom, a halogen atom etc.; R4 and R5 are the same or different and represent a hydroxyl group etc.; R6 and R7 are the same or different and represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms etc.; and R8 represents an optionally substituted cycloalkyl group having 3 to 7 carbon atoms etc.
CN1895246A Medicine for treating colpitis and cervical erosio A medicine for treating vaginitis and cervical erosion is prepared from ornidazole (20-80 Wt%) and borneol (20-80 Wt%).
US20100273728 Formulations For The Oral Administration of Therapeutic Agents and Related Methods The present application relates to an oral formulation of amphotericin B and other therapeutic agents, which formulation comprises one or more fatty acid glycerol esters and one or more PEG modified phospholipids or fatty acid esters. The formulation provides enhanced bioavailability and/or increased stability of the therapeutic agent at the low pH found in gastric fluid.
WO2014117710A1 Commands and method of treating cancer via rho pathway Lanosterol derivatives useful as anti-cancer agent, which can inhibit the growth of lung cancer cells, liver cancer cells, mammary cancer cells, brain cancer cells and pancreatic cancer cells, possibly by acting on the RHO pathway. These lanosterol derivatives are represented by compound LD030.
US20080287541 Kit for Treatment of Cancer The present invention relates to a kit for the treatment of cancer comprising (a) a container for containing a first compound (i) or a precursor thereof, said first compound or precursor being a compound that oxidizes glutathione (GSH); (b) a container for containing a second compound (ii) or a precursor thereof, said second compound or precursor being a compound that forms an adduct or conjugate with GSH; (c) a container for containing a third compound (iii) or a precursor thereof, said third compound or precursor being a compound that inhibits the rate-limiting enzyme of GSH biosynthesis, gamma-glutamylcysteine synthetase (GCS); and (d) a container for containing a fourth compound (iv) or a precursor thereof, said fourth compound or precursor being a compound that inhibits the enzyme responsible for the conversion of GSSG to GSH, glutathione reductase (GR).
CN103041040A Dong-nationality medical scraping-therapy preparation for treating lumbago and preparation method thereof The invention discloses a dong-nationality medical scraping-therapy preparation for treating lumbago and a preparation method thereof. The dong-nationality medical scraping-therapy preparation is prepared from the following raw materials in parts by weight as the basic prescription: 40-60 parts of aconite roots, 40-60 parts of radix aconite, 40-60 parts of paniculate swallowwort roots, 40-60 parts of peach seeds, 24-36 parts of lobedfruit tacca tuber, 40-60 parts of Japanese coniogramme rhizomes or herbs, 40-60 parts of radix angelicae, 40-60 parts of myrrh, 120-180 parts of camphor, 120-180 parts of borneol and 20-30 parts of menthol. Tea oil and bee wax are added to the basic prescription to prepare the preparation by decocting and mixing. The dong-nationality medical scraping-therapy preparation disclosed by the invention is dong-nationality medical scraping-therapy cream or scraping-therapy oil which is used by the dong-nationality. When the preparation is used for treating the lumbago, the therapeutic effect is strengthened, and the total effective rate is 99.9%.
EP2726086A2 Compositions containing nitro fatty acids Compositions, dietary supplement compositions, and topical compositions including activated fatty acids and methods for using activated fatty acids to treat a variety of diseases.
WO2013047889A1 Pharmaceutical composition for treating autoimmune diseases The purpose of the present invention is to provide a pharmaceutical composition and a treatment method both for treating/preventing autoimmune diseases. It is found that a pharmaceutical composition containing siRNA that can inhibit the expression of a CD98 heavy chain is useful for the prevention/treatment of autoimmune diseases. As a result, it becomes possible to provide a novel treatment method using the siRNA for autoimmune diseases such as type-1 diabetes and rheumatoid arthritis.
CA2345659C Biodegradable low molecular weight triblock polyester polyethylene glycol copolymers having reverse thermal gelation properties A water soluble, biodegradable ABA- or BAB-type tri-block polymer is disclosed that is made up of a major amount of a hydrophobic A polymer block made of a biodegradable polyester and a minor amount of a hydrophilic polyethylene glycol(PEG) B polymer block, having an overall average molecular weight of between about 2000 and 4990, and that possesses reverse thermal gelation properties. Effective concentrations of the tri-block polymer and a drug may be uniformly contained in an aqueous phase to form a drug delivery composition. At temperatures below the gelation temperature of the tri-block polymer the composition is a liquid and at temperatures at or above the gelation temperature the composition is a gel or semi-solid. The composition may be administered to a warm-blooded animal as a liquid by parenteral, ocular, topical, inhalation, transdermal, vaginal, transurethral, rectal, nasal, oral, pulmonary or aural delivery means and is a gel at body temperature. The composition may also be administered as a gel. The drug is released at a controlled rate from the gel which biodegrades into non-toxic products. The release rate of the drug may be adjusted by changing various parameters such as hydrophobic/hydrophilic component content, polymer concentration, molecular weight and polydispersity of the tri-block polymer. Because the tri-block polymer is amphiphilic, it functions to increase the solubility and/or stability of drugs in the composition.
US20110105413 Polymeric systems containing intracellular releasable disulfide linker for the delivery of oligonucleotides The present invention provides polymeric prodrugs including an intracellular releasable disulfide linker for the delivery of oligonucleotides. Methods of making the compounds as well as methods of delivering nucleic acids to tumor cells in a mammal using the same are also provided.
WO2007003964A1 G-protein coupled receptor agonists Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
CN101703463A Paracetamol temperature sensitive gel and preparation method and application thereof The invention relates to a paracetamol temperature sensitive gel and a preparation method thereof. The preparation is prepared by paracetamol, poloxamer solution and preservative and the like. The preparation of the thermosensitive gel is sensitive to the temperature, is flowable liquid at normal temperature, has reversible phase change closing to 33-37 DEG C of body temperature to form gel to directly act on administration position, thus not only being capable of being used for local administration, but also giving play to the function of treating the whole body through mucous membrane absorption; in addition, the preparation can conveniently and effectively be applied to body cavity mucous membranes and skin surfaces such as oral cavity, nasal cavity, rectum and vagina and the like, thus having antipyretic and analgesic functions. As the use dosage can be conveniently adjusted according to the needs of the patients, the preparation is suitable for bringing down a fever of infants rapidly, thus avoiding the problems of inconvenient administration by using the common formulations, such as paracetamol tabella and paracetamol turunda and difficult adjusting of dosage according to the needs of the patients.
US20120021044 Novel Cationic Lipid, A Preparation Method of the Same and A Delivery System Comprising the Same The present invention provides a novel cationic lipid, a preparation method of the same and a delivery system comprising the same. The cationic lipid of the present invention is used for the preparation of delivery systems of nucleic acids or physiologically active anionic proteins. The cationic lipid of the present invention can be conveniently prepared and purified by a simple process and is therefore economically highly advantageous for industrial-scale production thereof. Further, a nucleic acid or protein delivery system comprising the cationic lipid of the present invention not only significantly improves the intracellular delivery efficiency of desired nucleic acid drugs (such as DNAs, RNAs, siRNAs, antisense oligonucleotides, and nucleic acid aptamers) or anionic proteins having physiological activity, but also is usefully used to augment therapeutic efficacy of nucleic acid or protein drugs due to attenuated cytotoxicity of the delivery system.
EP1888518A1 Novel 8-sulfonyl-3 aminosubstituted chroman or tetrahydronaphtalene derivatives modulating the 5ht6 receptor The present invention relates to new compounds of formula (I), wherein R1 to R12, P, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
CN1977888B Medicinal composition of baicalin, ganoderma lucidum and salvia miltrorrhiza The present invention discloses a medicine composition and its preparation method. Said medicine composition is formed from (by weight portion) 50-1250 portions of baicalin, 500-24000 portions of ganoderma and 1000-90000 portions of salvia root. Said medicine composition also can be made up by using 50-1250 portions of baicalin, 7.5-360 portions of ganoderma polysaccharide and 30-1800 portions ofsalvia total phenolic acid. Said medicine composition can be made into various dosage forms, and can be used for curing various acute and chronic hepatitides.
US20110288148 Triggered covalent probes for imaging and silencing genetic expression The present invention relates to the use of cross-linking probes to covalently bind probes to nucleic acid targets. In some embodiments, the probe comprises an initiator region that is able to bind to a first portion of a target nucleic acid, a probe region linked too the initiator region that is able to bind to a second region of the target nucleic acid and that comprises one or more cross-linkers, and a blocking region hybridized to the probe region.
EP1869001A1 Substituted tetrahydroisochinolines as mmp inhibitors, related production method and use as medicine The invention concerns compounds of formula (I), wherein: at least one substituent R1, R2 or R3 represents an X-Q-Y group which enhances solubility, as well as the use of said compounds as medicines for preventing and/or treating diseases in which matrix metalloproteinases exhibit an increased activity.
CN1840171A Nutrition liquid for chronic nephropathy and preparation method thereof Disclosed is a nutrient solution for treating chronic kidney diseases and its preparing process, wherein each 500ml of the nutrient solution contains carbohydrate compound 55-65g, saturated fatty acid 10-12g, mono-saturated fatty acids 20-24g, protein 6-10g, zinc 5-10mg, ferrum 10-15mg, calcium 0.2-0.5g, cellulose 3-3.5g, complex vitamin B 10-30mg, active vitamin D 0.5-0.8ug, folic acid 1-2mg, vitamin C 50-100mg, pantothenic acid 3-5mg, yeast 10-15g, and probiotic 210-250mg.
CN1813936A Heat-clearing effervescence tablet for infants and its preparing method The present invention provides a Resuqing effervescent tablet for child and its preparation method. It is made up by using 625g of bupleurum root, 312.5g of scutellaria root, 625 g of isatis root, 312.5 g of pueraria root, 343.75 g of lonicera flower, 156.25 g of water buffalo horn, 375 g of forsythia fruit, 156.25 g of rhubarb and 125 g of lactose, 660 g of sodium hydrogen carbonate, 540 g of citric acid, 100 g of Aspatan, 100 g of polyethelene glycol 6000 and 4 g of magnesium stearate. Said effervescent tablet has obvious therapeutic effect for reducing fever.
US6924303 Analgesic and anti-inflammatory compositions containing COX-2 inhibitors The present invention is directed to an analgesic composition which consists essentially of a cyclooxygenase-2 inhibitor and a compound selected from the group consisting of non-steroidal anti-inflammatory drugs, acetaminophen and mixtures thereof. The present invention further is directed to a method for inducing analgesia through the administration of such a composition to a patient.
WO2010128443A1 Pyrrolidine-substituted flavones as radio-sensitizers for use in the treatment of cancer The present invention relates to a combination for the treatment of cancer wherein the combination exhibits a synergistic effect. The combination comprises radiation and at least one cyclin dependent kinase (CDK) inhibitor selected from the compounds of formula I or a pharmaceutically acceptable salt or a solvate thereof. The present invention also relates to a method for the treatment of cancer, which method comprises administering to a patient in need of such a treatment, a therapeutically effective amount of the combination. The present invention also relates to the use of a CDK inhibitor selected from the compounds of formula I as a radiosensitizer that enhances the efficacy of radiotherapy for the treatment of cancer, particularly head and neck cancer.
CN102697736A Cefixime granule and preparation method thereof The invention relates to the field of pharmaceutical preparations, especially to a cefixime granule and a one-step granulating method of the cefixime granule. The cefixime granule comprises the following components by weight: 1-20% of cefixime, 56-95% of diluent, 0.5-1.0% of a buffer agent, 0.5-10% of adhesive and 0.1-5% of flavoring. The cefixime granule has the advantages of good quality stability, good suspension property and good content uniformity, and good taste simultaneously, so that the cefixime granule is especially suitable for children and crowd of dysphagia, and medication compliance is good. A preparation method of the cefixime granule further is provided by the invention; due to use of the one-step granulating method, steps of mixing, granulating and drying are finished in the same one fluidized bed by one step; operation method is simple, and production efficiency is high, so that the preparation method is especially suitable for industrial production.
US6906203 Anticancer agents; such as 2-Amino-3-cyano-4-(2-bromo-4,5-dimethoxyphenyl)-4H-indolo(4,5-b)pyran The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, Z and R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
WO2010146055A1 Antagonists of beta-catenin for preventing and/or treating neurodegenerative disorders The invention relates to antagonists of β-catenin for use in the prevention and/or treatment of neurodegenerative disorders, β-catenin has been found to specifically accumulate in Huntington's disease and this accumulation is toxic in striatal neuron expressing mutant huntingtin, the causal protein of Huntington's disease. Since β-catenin had been previously reported to accumulate in Alzheimer's disease, interfering with β-catenin accumulation in neuronal cells provides a therapeutic approach for the prevention and/or treatment of neurodegenerative disorders.
CA2595711A1 Methods and compositions using 4-amino-2-(3-methyl-2,6-dioxopiperidin-3-yl)-isoindole-1-3-dione This invention relates to racemic and stereomerically pure 4-amino-2-(3-methyl-2,6-dioxopiperidin-3-yl)-isoindole-1,3-dione, and prodrugs, salts and solvates thereof. Synthesis, methods of use, and pharmaceutical compositions of racemic and stereomerically pure 4-amino-2-(3-methyl-2,6-dioxo-piperidine-3-yl)-isoindole-1,3-dione, and prodrugs, salts and solvates thereof, are disclosed.
US20100227909 Compositions comprising mir34 therapeutic agents for treating cancer In one aspect, the invention generally relates to compositions comprising miR-34 and siRNAs functionally and structurally related to miR-34 for the treatment of cancer.
DE102006053500A1 Antimicrobial compounds for controlling selective microorganisms such as gram-positive bacteria, particularly coryneform bacteria, has general formula The compound has a general formula (I). The compound having the formula (I), is new. R 1 to R 4H, hydroxy groups, alkyl groups, 1-10C hydroxyalkyl group; R 5H, 1-4C acyl group; AO : residue selected from -CH 2CH 2O, -CH 2CHR 6O, -CHR 6CH 2O, -CH 2CH 2OHCH 2O, where R 6=1-4C alkyl; and n : 1-20. Provided that: (A) R 3 and R 4 are not H at the same time; (B) sum of C atoms in R 3 and R 4 is not greater than 18; and (C) sum of C-atoms in R 1, R 2, R 3 and R 4 does not exceed 36. [Image] - ACTIVITY : Antimicrobial; Antiseborrheic; Dermatological. 20 ml of a 0.3 wt% solution of test substance i.e. lactic acid octylamide and lactic acid hexylamide in water was inoculated with 200 microliter of a refined 48 hour-culture of Corynebacterium xerosis or Staphylococcus epidermidis and was incubated for 3 days at 37 deg C. 1ml of each sample was extracted at a period of 1, 3, 24 and 48 hours and the bacterial count was determined. The test substance lactic acid octylamide used with the microorganism C.xerosis showed 9.1E + 5 colony forming unit (CFU)/ml at 0 hours, 3.0E + 6 CFU/ml after 3 hours and less than 2.0E + 2 CFU/ml after 48 hours, which clearly showed decrease in the colony formation of the microorganism. - MECHANISM OF ACTION : None given.
EP2624839A1 Composition for use in the treatment of acne A composition comprising from 10 to 15 % by weight of sucrose palmitate which may be used in the treatment of acne.
US6903083 Stabilized hydroxyvitamin D The invention provides a stabilized 1α-hydroxyvitamin D (“SHVD”) which is particularly well suited for pharmaceutical formulations.
CN101416969A Preparation method of ecdysterone cream capable of promoting wound healing The invention provides a preparation method of a cream preparation which can quicken wound healing. The components of the cream preparation comprise: glycerol monostearate, stearic acid, white Vaseline, azone, ethylparaben, purified water, borax, lauryl sodium sulfate, triethanolamine, glycerin, allantoin, ecdysterone and ethanol, wherein, the primary active ingredient is the ecdysterone which can significantly promote the proliferation of endothelial cells, epithelial cells and fibroblasts, and the mechanism thereof is that the ecdysterone can promote the synthesis of proteins and trigger the synthesis of DNA of cells. The cream preparation has the advantages of no anaphylaxis, no irritation, easy absorption, obvious therapeutic effect, low price, convenient carrying and the like. In addition, experiments validates that the cream preparation does have the efficiency of healing wounds. The cream preparation is similar to Yunnan white drug powder and also varies from the Yunnan white drug powder in the therapeutic effect.
CN102247389A New use of Echinacoside in sleep deprivation The invention relates to new use of Echinacoside in sleep deprivation. A mat sleeping model is built by a small platform environment process, and the reactivity and learning ability of a mat are detected by a Morris labyrinth and a mat diving platform. Results show that the Echinacoside can obviously improve ethology in rats after sleep deprivation. The Echinacoside can obviously improve the ethology in rats after sleep deprivation.
US20110009494 Inhibition of the Survival of Pancreatic Cancer by Cyclohexenone Compounds from Antrodia Camphorata The present invention relates to a novel application of a compound. The compound 4-hydroxy-2,3-dimethoxy-6-methyl-5-(3,7,11-trimethyl-dodeca-2,6,10-trienyl)-cyclohex-2-enone of the invention is isolated and purified from the extracts of Antrodia camphorata, which can be applied for inhibiting the survival of pancreatic cancer cells and be used as a pharmaceutical composition to inhibit the pancreatic tumor growth.
WO2005117878A1 Irinotecan preparation An irinotecan preparation having irinotecan and/or a salt thereof highly carried by a closed vesicle carrier, which exhibits a strikingly prolonged retention in blood as compared with that of conventional irinotecan liposome preparations and is capable of being present in blood for a prolonged period of time. There is provided an irinotecan preparation comprising closed vesicles formed of a lipid membrane wherein irinotecan and/or a salt thereof is sealed in a concentration of at least 0.07 mol/mol (medicine mol/total membrane lipid mol). The irinotecan preparation preferably has an ion gradient between an inner water phase and an outer water phase within the closed vesicles. The closed vesicles are preferably liposomes, and the liposomes preferably have only the external surface thereof modified with a surface modifier containing a hydrophilic polymer.
US20110123619 Buccal delivery system A buccal delivery system capable of being blended in a normal dry powder process and compressed using a standard tabletting machine, said buccal delivery system comprising a matrix of: (a) an effective amount of one or more active ingredients; (b) an amount of one or more polyethylene glycols or derivatives thereof having a molecular weight between 1000 to 8000 sufficient to provide the required hardness and time for dissolution of the matrix; (c) 0.05-2% by weight of the total matrix of one or more suspending agents; (d) 0.05-2% by weight of the total matrix of one or more flowing agents; and (e) 0.05-2% by weight of the total matrix of one or more sweeteners.
US20100168194 Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone Compounds For The Inhibition Of Beta-secretase The present invention provides compounds and methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
CN101343265B Extraction method of effective ingredients of cave flower The invention discloses a medicine prepared by an active ingredient C18H16O7 extracted from stone flower. The invention provides a preparation method which mainly adopts solvents such as petroleum ether, normal hexane and ethyl acetate for extraction, and selects the solvents with large polarity to remove coloring matters, and adopts the solvents with small polarity for recrystallization, so as to prepare the active ingredient of C18H16O7. The medicine and the preparation method have advantages of low active ingredient loss, high crystallization purity, stable product yield, good quality and reasonable process. A quality detection method provided in the invention can properly control the product quality and ensure the related drug effects of products, more specifically, the invention relates to a pharmaceutical preparation made by the active ingredient of stone flower and derivates thereof and having the related regulating actions of anti-inflammation, anticancer, antivirus and prevention and cure of hypoimmunity.
US20080076800 Anticancer, inflammation, arthritis, angiogenesis, neurodegenerative diseases, fungal infections, malaria; Heat-shock protein 90 inhibitors; 4-(6,6-Dimethyl-4-oxo-3-methyl-4,5,6,7-tetrahydro-indazol-1-yl)-2-(3,4,5-trimethoxyanilino)-benzamide Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein A, Q1, Q2, Q3, R3, R4, R5, RO, m, and p are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
WO2006009209A1 Preventive or therapeutic agent for chronic inflammatory lung disease Not only acute or chronic interstitial hepatitis and lung fibrosis but also chronic obstructive lung diseases, such as lung emphysema and chronic bronchitis, can be effectively prevented or treated by inhalation administration to the lung tissue of 2-{N-[4-(4-chlorobenzenesulfonylamino)butyl]-N-{3-[(4-isopropyl-2-thiazolyl)methoxy]benzyl}}sulfamoylbenzoic acid or a pharmacologically acceptable salt thereof.
EP2316820A1 2-aryl-propionamide derivatives useful as bradykinin receptor antagonists and pharmaceutical compositions containing them (R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.
USRE39433 Therapeutic agents as cytokine antagonists and agonists A therapeutic agent capable of of binding to the F′-G′ loop of domain 4 of the common c Chain of the receptor for GM-CSF, IL-3, and IL-5. The amino acid Tyr421 which is located in the F′-G′ loop is critical in the high affinity binding and stimulation of function of GM-CSF, IL-3 and IL-5 to the common c chain of the receptors. Other receptors for cytokines also show hydrophobic amino acids in analogous positions and it is probable that they too play a pivotal role in binding of respective cytokines to them and in modulating function. Agents capable of binding to the F′-G′ loops are suggested and should be of therapeutic value.
CN101856377A Compound preparation for treating nephrotic syndromes The invention relates to a compound preparation for treating nephrotic syndromes. A capsule of the compound preparation is prepared by combining 400 milligrams of ginsenoside and 10 to 20 milligrams of prednisone or 8 to 16 milligrams of meprednisone. The compound preparation not only enhances the biological effect of hormones, but also reduces the side effect of the hormones, so that the progress of the state of illness can be controlled more effectively. The compound preparation utilizes the effects of stress resistance, inflammatory resistance and the like of the ginsenoside used as main active ingredients of panax ginseng fully, has the two-way adjusting effect on the immunologic function and particularly has the synergistic effect on the prednisone, and is widely suitable for the treatment of autoimmune diseases.
EP0866874B2 Process for the preparation of materials with a high content of isomers of conjugated linoleic acid Organic materials, comprising a mixture of at least two products (I) and (II), both containing isomers of conjugated long chain polyunsaturated fatty acids moieties (L1) and (L2) can be obtained by subjecting an organic material, selected from free fatty acids, mono-, di- or triglycerides, phospholipids, alkylesters or wax-esters, containing at least 5 wt.% of these conjugated polyunsaturated fatty acids, to an enzymic conversion (acidolysis, alcoholysis, esterification, hydrolysis) using an enzyme that can be discriminated between (L1) and (L2), so that original ratio L1/L2 = XA in starting material is increased to XB, wherein XB ≥ 1.1 XA.
US20120157528 Leave-on nonsolid skin conditioning compositions containing 12-hydroxystearic acid and ethoxylated hydrogenated castor oil Leave-on non-solid skin conditioning compositions comprising 12-hydroxy stearic acid. Compositions contain 12HSA, yet have a relatively low viscosity, so are suitable for spreading on the skin, and are stable on storage and structurally reversible through temperature cycling.
CN103087061A Substituted purrocoline compound and preparation method and application thereof The invention discloses a substituted purrocoline compound shown as a formula (I) and a preparation method and application thereof. The definition of each substituent group in the formula (I) is detailed in the specification. The experimental data proves that the compound has the function of inhibiting the VIF (virus infection factor) activity due to the interaction of inhibiting VIF/ElonginC and has the function of inhibiting virus replication. The compound with the acting mechanism is expected to reduce the tolerance problem in the HIV (human Immunodeficiency virus) treatment process, and a novel medicine is provided for treatment of a HIV patient.
US20100076089 Antimicrobial gel formulations Disclosed herein are formulations comprising an N-halogenated or N,N-dihalogenated amine compound dispersed in a water-swellable polymer, wherein the compound is 90% stable for at least 30 days at about 25° C. Also disclosed are methods of treating or preventing infections caused by a bacterial, a microbial, a sporal, a fungal or a viral activity using such formulations.
WO2007045877A1 4-heteroarymethyl substituted phthalazinone derivatives 1.A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from formula (i), where Y1 is selected from CH and N , Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and formulae (ii), (A) and (B) where Q is O or S; RD is formula (C) wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C=O; RN2 is selected from H and optionally substituted C1-10 alkyl; Rc3 and Rc4 are independently selected from H, R, C(=O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRc1Rc2; RC1 and RC2 are independently selected from H, R, C(=O)OR, where R is optionally substituted C1 -10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, s uch that there is a double bond between the atoms substituted by RC1 and RC3.
CN101485749B Effervescent tablets for women as well as preparation method and application thereof The invention relates to an external gynaecological inflammation clean effervescent tablet with antibiotic activity, a method for preparing the same and application thereof. The effervescent tablet is prepared from rhizoma coptidis, pomegranate bark, coral, litharge, sodium bicarbonate, polyethyleneglycol 6000, citric acid, lactose, polyvinylpyrrolidone, magnesium stearate and superfine silica gel powder, and has the advantages of clearing heat and drying damp, killing insects and relieving itching, giving a play to strong inhibition on woman vagina pathogen, high safety and good stability, and having no obvious toxic side effects and drug resistance as well as convenience to use, carry and store by a patient. The effervescent tablet is applied to treating various gynaecological diseases of colpitis, vulvitis, and the like caused by infusorium, fungi and bacteria, and can be used as a preventive medicine for long term usage simultaneously.
CN103536605A Application of anti-human immunodeficiency virus (HIV) drug amprenavir in preparation of antitumor drug The invention discloses application of anti-human immunodeficiency virus (HIV) drug amprenavir in preparation of an antitumor drug. The anti-HIV drug amprenavir identified by food and drug administration (FDA) is taken as a material; the killing effect of the amprenavir on a tumor cell is detected by adopting a microwave theory and techniques (MTT) method. An experiment proves that the amprenavir has a significant inhibiting effect on multiplication of a plurality of tumor cells, such as a breast cancer michigan cancer foundation (MCF-7) cell, a non-small cell lung cancer A549 cell, a mouse embryonic fibroblast glioblastoma multiforme L929 cell, a colon cancer HT29 cell, a brain glioma U87 cell and the like, so as to clarify new use of an old drug. Therefore, foundation is provided for development of a novel anti-tumor drug.
WO2013045607A1 Quinazoline linked heteroaromatic tricycle derivatives as pde10a enzyme inhibitors This invention is directed to compounds of formula I which are PDE10A enzyme inhibitors, pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier and processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder, a drug addiction or a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. Formula I, wherein Q is selected from the group consisting of (Q1), (Q2), (Q3), (Q4), and (Q5).
WO2013033370A1 Prevention and treatment of thrombosis in medically ill patients Provided herein are methods for preventing and treating thrombosis in medically ill patients by administering to the patient a therapeutically effective amount of betrixaban.
CN102697774A New application of Korean mondshood root total alkaloids and guanfu base VIIII The invention provides a preparation method of Korean mondshood root total alkaloids and applications in preparing a slow sodium-ion passage blocking agent and preparing drugs for resisting arrhythmia. Both the Korean mondshood root total alkaloids and the guanfu base I are provided to have an effect for inhibiting slow sodium current of ventricular muscles of cavies. The invention particularly relates to an application of guanfu base VIIII in preparing a drug-metabolizing enzyme inhibitor. The invention also provides an application of guanfu base VIIII in preparing a slow sodium-ion passage blocking agent.
CN102266325B Melbine crystal and medicinal composition of melbine and saxagliptin and preparation method thereof The invention discloses a melbine crystal and a medicinal composition of melbine and saxagliptin and a preparation method thereof. The medicinal composition consists of active ingredients of medicines and a pharmaceutic adjuvant, wherein the active ingredients of the medicines comprise the following components in part by weight: 5 to 30 parts of saxagliptin and 200 to 800 parts of melbine, and the melbine is the melbine crystal; and the pharmaceutic adjuvant comprises a filling agent, a disintegrating agent, an adhesive and a lubricating agent. The melbine crystal used in the medicinal composition has the characteristic of low solubility, so the sustained-release effect of the melbine is realized by using ordinary matrix materials in the medicinal composition prepared from the melbine andthe saxagliptin, the administration safety is improved; and the synergistic effect of the melbine and the saxagliptin is good, so the curative effect is improved. In addition, due to the adoption of few matrix materials, the stability of the medicines is improved.
US20080200474 Novel flunarizine salt forms and methods of making and using the same Disclosed herein are novel salts of flunarizine with improved properties. Also described herein are novel pharmaceutical compositions comprising such flunarizine salts, methods of making, and related methods of treatment.
EP1339694B1 Substituted 2-phenylaminoimidazoline phenyl ketone derivatives as ip antagonists This invention relates to compounds which are generally prostaglandins I2 (IP) receptor modulators, particularly IP receptor antagonists, and which are represented by the general formula (I) wherein A, R?1 and R2¿ are defined in the specification; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, a process for the preparation of such compounds and their use for treating diseases associated with pain, inflammation, urinary tract disease states, respiratory disease states, edema formation, or hypotensive vascular diseases.
WO2014045072A3 Deuterium depleted water and/or deuterium-depleted organic compound for the treatment of hypertension The main subject of the invention is a pharmaceutical composition comprising deuterium depleted water (DDW) and/or deuterium-depleted organic compound (DDOC) for use as hypertensive agent, wherein the D-content of the DDW or DDOC is 0.01 to 135ppm, and optionally the composition comprises auxiliary materials and optionally the composition comprises other known antihypertensive agent. Another important subject of the invention is an aqueous pharmaceutical composition for use as antihypertensive agent, where the aqueous component of the composition is deuterium depleted water (DDW), wherein the D-content of the DDW is 0.01 to 135 ppm.
WO2005121112A1 Medicinal compositions containing 6-hydroxybenz- bromarone or salts thereof [PROBLEMS] To provide highly safe therapeutic or preventive agents for hyperuricemia, more specifically uricosuric agents, which have potent uricosuric effect and do not cause grave hepatopathy. [MEANS FOR SOLVING PROBLEMS] Medicinal compositions for the treatment or prevention of hyperuricemia or diseases caused by hyperuricemia, which contain 6-hydroxybenzbromarone or salts thereof, and pharmaceutically acceptable carriers; uricosuric agents, xanthine oxidase inhibitors, and inhibitors against the uptake of uric acid in kidney, which contain 6-hydroxybenz- bromarone or salts thereof; and a process for the production of 6-hydroxybenzbromarone.
CN1850158A Tanshinoue dropping pills and preparing method The present invention provides a kind of tanshinone dripping pills. It is made up by adopting the following steps: using ethyl alcohol to extract salvia root to obtain tanshinone extract, then mixing said tanshinone extract with matrix and making them into dripping pills. Said tanshinone dripping pills can be used for curing various inflammations, such as osteomyelitis, acne, tonsillitis, mastitis and others.
US20050032806 Method for treating anhedonia using dopamine agonists A method of treating anhedonia in a patient in need thereof, comprising administering to the patient an effective amount of a dopamine agonist
WO2007066181A2 Methods of preparing a vegf-r inhibitor The present invention relates to methods for preparing a compound of formula (7), which is useful as a modulator and/or inhibitor of protein kinases. The present invention also relates to intermediate compounds useful in the preparation of a compound of formula (7).
US7268152 Antiinflammatory agents; antiallergens; antiproliferative agents Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
US20110172198 TGR5 Modulators And Methods Of Use Thereof The invention relates to compounds of Formula A: (A) or a salt, solvate, or hydrate thereof. The compounds of formula A are TGR5 modulators useful for the treatment of disease.
US20080312310 Compounds, Compositions and Methods Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders, for example, by modulating the activity of KSP, are disclosed.
US20110189161 Nutrigenomics methods and compositions The present invention provides a proprietary compositions and systems to modulate genetic and metabolomic contributing factors affecting disease diagnosis, stratification, and prognosis, as well as the metabolism, efficacy and/or toxicity associated with specific vitamins, minerals, herbal supplements, homeopathic ingredients, and other ingredients for the purposes of customizing a subject's nutritional supplement formulation to optimize specific health outcomes. Specific to this invention the utilization of certain known polymorphic genes associated with Substance Use Disorder (SUD) are analyzed to target certain genetic anomalies that lead to a high risk and predisposition to SUD. The genotypic patterns are then utilized to provide certain nutritional customized solutions especially related to the attenuation of aberrant abuse of physician prescribed narcotic pain medication across all pain conditions. A priority GENOPROFILE is measured and directs the customization of a subsequent nutraceutical to act as a therapeutic modality. Specifically the treatment includes slow attenuation of the pain medication by incorporating orals (shakes, liquid beverages, pills, tablets, troche, ointments etc.), Intramuscular, Intravenous, intra-rectal and any form necessary to deliver a sufficient amount of an anti-craving and anti-stress nutraceutical. Moreover, the invention includes examples of novel analgesic ointments coupling Synaptamine and such analgesic and other anesthetic compounds including but not limited to Gabapentin, Ketamine, Baclofen, Ketoprofen, Amitriptyline, Lidocaine, Cyclobenzapine, Diclofenac, Menthol, Camphor and Capsaicin. The GENOPROFILE will be used to determine pain sensitivity Intolerance.
CN101669955A Pharmaceutical composition for treating respiratory diseases The invention relates to an oral preparation pharmaceutical composition for treating respiratory diseases, which comprises effective doses of ambroxol, cefixime, a corrigent and other pharmaceuticallyacceptable adjuvant materials.
CN101234992A Method for preparing aspartic acid A preparation method of potassium aspartate belongs to chemical field, which is characterized in that the invention adds potassium salt and aspartic acid into water to be reacted, removes part or all water, and adds residues into soluble non-aqueous solvent to precipitate solid to be broken and dried to obtain final product. Compared with prior art, the preparation method of potassium aspartate can improve product yield, reduce production cost, improve production efficiency and improve product quality.
US20080008740 Pharmaceutical Composition for Rectal, or Vaginal Application, Method of Manufacturing and Use as Medicament Thereof A pharmaceutical composition for rectal or vaginal application, characterized in that it contains as active substance the platinum complex of general formula wherein A each independently is an —NH3 group or an amino group containing 1 to 18 carbon atoms, B each independently is a halogen atom, a hydroxy group or a —O—C(O)—R group wherein R each independently is hydrogen atom or an alkyl, alkenyl, aryl, aralkyl, alkylamino or alkoxy group containing 1 to 10 carbon atoms or functional derivatives of these groups, and X each independently is a halogen atom or a monocarboxylate group containing 1 to 20 carbon atoms, or X together form a dicarboxylate group containing 2 to 20 carbon atoms, and a hydrophilic gel-forming base, comprising gelatin, water and glycerol.
CN101190256A Chuanqisan for treating cervical spondylopathy and preparation method The invention discloses a szehuan lovage root powdered medicine used for treating cervical spondylosis and the preparation method thereof, which is prepared according to proportion by tortoise plastron, suberect spatholobus stem, Danshen root, radix astragali, angelica, fortune's drynaria rhizome, eucommia bark, pyrite, szechuan lovage rhizome and himalayan teasel root processed respectively in advance. The invention has the functions of invigorating qi, activating blood circulation, soothing the veins, eliminating stasis and relieving pain. The medicine disclosed by the invention has the advantages of high curative effect, rapid effectiveness show, no toxic and side effect and low cost.
WO2007126913A1 Methods for prevention or treatment of viral disease Compositions and methods are provided for preventing or treating viral disease and other related diseases in a mammalian subject. The method provides administering to the mammalian subject a compound capable of inhibiting a TEC tyrosine kinase, wherein the compound is administered in an amount effective to reduce or eliminate the viral disease or to prevent its occurrence or recurrence. A method for identifying a compound capable of inhibiting viral infection of a cell is provided wherein the compound is a TEC tyrosine kinase inhibitor.
CN102988988A Pharmaceutical composition for treating pulmonary aspergillosis The invention provides a pharmaceutical composition for treating pulmonary aspergillosis. The effective components of the pharmaceutical composition comprise the pulmonary aspergillus allergen vaccine and the anti-fungal agent. The pharmaceutical composition can be used for treating the pulmonary aspergillosis by inhibiting the growth of the aspergillus effectively and can be also used for eliminating and reducing the organism damage and the clinical symptoms which result from the allergic reaction caused by the aspergillus allergen.
WO2009157586A1 Transdermal patch containing fentanyl or salt thereof Provided is a patch containing fentanyl or a derivative thereof which causes no lowering in the stickiness to the skin, has a high drug-stability, can inhibit the time-dependent deposition of fentanyl crystals, yet little irritates the skin and shows an extremely high skin permeability of fentanyl. A patch containing fentanyl or a derivative thereof consisting of a support, a pressure-sensitive adhesive layer containing fentanyl or a derivative thereof and a release liner, wherein the pressure-sensitive adhesive layer containing fentanyl or a derivative thereof contains 0.01 to 0.5% by mass of an ascorbate such as an L-ascorbate palmitate. A patch containing fentanyl or a derivative thereof which further contains a hindered phenol-type antioxidant in an amount sufficient for the inhibition of the deposition of fentanyl or a salt of the same.
US20080096940 5-Hydroxy-Benzothiazole Derivatives Having Beta-2-Adrenoreceptor Agonist Activity Compounds of formula (I) in free or salt or solvate form, wherein T has the meaning as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the β2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
CN101259098A Long-acting low molecule heparin intraocular sustained-release system The invention relates to an ophthalmic controlled release system of long-action low molecular heparin which comprises the low molecular heparin as drug and a drug carrier made from synthesized or natural biodegradable high molecular materials and is characterized in that the proportion range of the low molecular heparin and the drug carrier is (1:8) to (5:1); the average molecular mass of the low molecular heparin is less than 8000 Dalton; the molecules less than 8000 Dalton, the salt compounds of the low molecular heparin such as sodium salt, calcium salt and kali salt included, take up not less than 60 percent of the total molecules of the low molecular heparin; the synthesized or natural biodegradable high molecular materials are polyglycolic acid and gelatin or bletilia striata gelatin respectively. The ophthalmic controlled release system of long-action low molecular heparin can effectively inhibit the proliferation and migration of lenticular epithelia and fibroblasts in eyes, reduce fibrinous exudates post operation, alleviate inflammatory reaction post operation and prevent posterior capsular opacification, thereby inhibiting the occurrence of after-cataract; meanwhile, the ophthalmic controlled release system of long-action low molecular heparin inhibits the proliferation of retinal pigment epithelium and fibroblasts, thus inhibiting the proliferative vitreoretinopathy (PVR).
CN101766817A Medicine carrier and application thereof The invention discloses a medicine carrier and the application thereof. An active ingredient of the provided medicine carrier is a Nano particle with positive charge. The Nano particle is formed by a triblock copolymer of MPEG (methoxy polyethylene glycol)-polycaprolactone-polyphosphonate. The invention further provides medicine for treating cancer, and the active ingredient of the medicine is the Nano particle which is formed by the MPEG-polycaprolactone-polyphosphonate loading with anti-cancer medicine. As a cation type amphiphilic segmented copolymer with biocompatibility, the triblock copolymer of MPEG-polycaprolactone-polyphosphonate forms the Nano particle with positive charge and a hydrophobic core in water solution in a self-assembly manner; the stability is good, the preparation method is simple, and the repeatability is high; the hydrophobic anti-cancer medicine can be loaded into the hydrophobic core and can be combined with siRNA with negative charge, so as to form a medicine feeding system which can convey the anti-cancer medicine and the siRNA at the same time. The medicine carrier and the medicine in the invention not only have great social and economic benefits, but also have good application prospect.
US20090053203 Chimeric metal binding protein for use in prevention and treatment of cancer, diabetes, obesity, cardiovascular, metabolic, neurodegenerative, gastrointestinal, autoimmune, rheumatological and infectious diseases; drug delivery The present invention is related methods of delivering MBD peptide-linked agents into live cells. The methods described herein comprise contacting MBD peptide-linked agents to live cells under a condition of cellular stress. The methods of the invention may be used for therapeutic or diagnostic purposes.
WO2007150002A2 PRODRUGS OF 5-AMINO-3-(3'-DEOXY-β-D-RIBOFURANOSYL)-THIAZOLO[4,5-d] PYRIMIDIN-2,7-DIONE The invention is directed to 5-amino-3-(3'-deoxy-β-D-ribofuranosyl)-thiazolo[4,5-d]pyrimidin-2,7-dione prodrugs, whose metabolized parent compound has immunomodulatory activity. The invention also relates to the therapeutic use of such prodrugs and pharmaceutical compositions thereof in treating disease states associated with abnormal cell growth, such as cancer.
US20080076819 Treating non-insulin dependent diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome; 6-[(1-cycloheptyl-4,4-dimethyl-5-oxopyrrolidin-3-yl)methoxy]nicotinonitrile for example A compound of formula (I): or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Methods of inhibiting 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. Methods of treating non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
WO2012105562A1 Novel macrolide derivative The inventors have successfully obtained a compound having josamycin as the lead mother nucleus and having excellent antibacterial activity against the causative bacteria of respiratory tract infection in animals.
US20120095418 Self-Supporting Films For Delivery Of Therapeutic Agents The present disclosure relates to self-supporting films for delivery of a therapeutic agent containing at least one hydrophobic polymer and at least one therapeutic agent. Methods of forming the self-supporting films are also disclosed.
CN1923228B Pharmaceutical composition comprising notoginseng extract, Danshen extract and ligustrazine The invention belongs to the field of pharmacy, and discloses a medicinal composition containing pseudo-ginseng extract, red sage root extract, ligustrazine or pharmaceutically acceptable salts, which can be used for treating cardiovascular and cerebrovascular diseases, the invention also discloses the preparation containing the pharmaceutical composition and its preparing process, wherein the constituents include (by weight ratio) pseudo-ginseng extract 30-400 parts, red sage root extract 10-400 parts, ligustrazine or its pharmaceutically acceptable salts 10-400 parts, the composition can beprepared into any clinically or pharmaceutically acceptable dose forms, preferably injections.
US7081258 Composition for promoting hair growth The present invention relates to a composition for promoting hair growth. More particularly, the present invention comprises a component for inhibiting 5α-reductase activity, a functional component of cell activity, and an expansion component of peripheral blood vessels. A composition for promoting hair growth of the present invention has a superior effect on hair growth.
CN102580097A Medicinal composition containing azilsartan The invention relates to a medicinal composition containing azilsartan. The medicinal composition contains azilsartan, hydragogue and pharmaceutically-acceptable auxiliary materials. According to the medicinal composition, the azilsartan has the superiority in a dissolving-out aspect and has an obvious synergistic effect under the condition of combining the azilsartan and the hydragogue, and the dose can be reduced.
CN101455675B Ferulaic acid and astragaloside combination for treating and preventing renal interstitial fibrosis, and preparation method and use thereof The invention discloses a composition with the function of preventing and/or treating renal interstitial fibrosis. Components thereof are ferulic acid and astragaloside IV with 1:5-5:1 of weight ratio. The composition is made by mixing the ferulic acid and the astragaloside IV, has the similar kidney protecting function of preventing and treating renal interstitial fibrosis to angiotensin converting enzyme inhibitors (ACEI), can be used to prepare drugs for preventing and/or treating renal interstitial fibrosis, and also can be used as auxiliary agent for drugs for preventing and/or treating renal interstitial fibrosis.
WO2006066955A1 Quinoline derivative, use and production thereof, and drug containing the same The invention relates to a quinoline derivative of general formula (A), wherein R1, R2, R3, X, Y, Z and A are defined as in the description and the claims. The invention also relates to the use of the compounds of general formula (A) in the treatment of various diseases and to the production of the compounds of general formula (A).
WO2009060281A3 Immune stimulatory oligoribonucleotide analogs containing modified oligophosphate moieties lmmunostimulatory oligoribonucleotides (ORN) featuring 5'-triphosphates and various 5'-triphosphate analogs are provided. Also provided are physiologically acceptable salts of the immunostimulatory ORN and pharmaceutical compositions containing the immunostimulatory ORN of the invention. ORN of the invention are useful as adjuvants and can be combined with an antigen to promote an antigen- specific immune response. ORN of the invention are also particularly useful for promoting a Th1 -type immune response. Also provided are methods of use of the compounds and pharmaceutical compositions of the invention to enhance an immune response in a subject, as well to treat a number of conditions including cancer, infection, allergy, and asthma, and to vaccinate a subject against an antigen.
CN103690534A Application of prodiginine (PG) in prevention and control of bombyx morinuclear polyhedrosis virus The invention relates to the effect of small molecule compound prodiginine (PG) for inhibiting BmNPV (bombyx mori nuclear polyhydrosis virus), and application thereof in prevention and control of BmNPV. Cell assay indicates that PG can interfere with proliferation of BmNPV in cells in a concentration range of 0.01-0.8 mu g/L to stop formation of virus polyhedron, and can selectively cause death of silkworm cells infected with BmNPV in a concentration range of 1-300 mu g/L with the death rate being over 97 percent; PG does not show toxicity to normal cells of silkworm in the application ranges. Individual tests indicate that the silkworms infected with BmNPV stop taking food and prematurely die, infected silkworms can be removed easily, and prodiginine does not show toxicity to healthy cells when prodiginine is used for orally feeding silkworm in a concentration range of 1-10mg per silkworm. Proliferation of BmNPV and formation of polynedron can be inhibited by utilizing PG, and PG has the effect of accelerating death of BmNPV, and can prevent and effectively control spread of BmNPV.
US20080269341 administering to patient fenretinide for treating an infectious disease, or bone disease osteopenia or osteoporosis; decreasing arachidonic acid levels, increasing docosahexaenoic acid; for increase osteoblast formation; diagnostic and screening disease based on the lipid level The present invention relates to methods for the treatment of a disease or condition associated with lipid imbalance, comprising (a) decreasing arachidonic acid (AA) levels, (b) increasing docosahexaenoic acid (DHA) levels, (c) increasing DHA/AA ratio or (d) any combination of (a)-(c) in a subject using fenretinide. The invention also relates to diagnostic and screening methods based on the determination of lipid levels.
EP1289533B1 Whitening compositions containing ascomycete derived enzyme The present invention relates to topical whitening compositions comprising a whitening effective amount of an Ascomycete-derived melanin-degrading enzyme extract and methods of preparing the composition. The composition provide a whitening effect which occurs by degrading melanin in the skin, yet the compositions themselves do not turn dark in color. The enzyme extract can be derived from Aspergillus fumigatus or Saccharomyces cerevisiae, and is added to the compositions of the present invention. The compositions containing the enzyme extract are twice as effective as kojic acid in producing a whitening effect on the skin.
WO2010070060A1 Bicyclic pyrazoles as protein kinase inhibitors 3,4-diaryl-bicyclicpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
EP2651425A1 Algal extract-based composition for oro-dental use An algal extract-based composition for oro-dental use is provided. This composition comprising a mixture of algae with at least Ascophyllum nodusum and Fucus spp, is characterized in that said mixture of algae has a proportion of Ascophyllum nodusum of at least 90% of the weight of the mixture and that the proportion of Fucus spp. is at most 10% of the weight of the mixture, and in that said extract is combined with a natural surfactant and/or with a zeolite or a mixture of zeolites. Uses of said composition, in particular tot dental prevention and or care are also provided. Applications in the oro-dental field, both preventively and curatively.
CN101502490A Ketoprofen bioadhesive gel microsphere and preparation method thereof The invention discloses a ketoprofen bio-adhesive gel microsphere preparation and a preparation method thereof. The microsphere comprises ketoprofen and a drug carrier, wherein, the drug carrier thereof is calcium pectinate formed by mixing a polysaccharide solution and a CaCl2 solution with the proportion of polysaccharide to drugs being (1:1) to (1:6); the concentration of the CaCl2 solution is0.5% to 20%; and the concentration of the polysaccharide solution is 5%. By preparing the gel microsphere on the basis of the dropping preparation method, the prepared microsphere has the advantages of smaller grain diameter, good sphericity, high entrapment rate and higher drug-loading rate, and the microsphere has good sustained-release effect under the bio-adhesive action; the preparation method has the advantages of mild preparation process, easy operation and simple steps; the carrier of the gel microsphere, as a natural high-polymer polysaccharide substance, has high biocompatibility and minimizes the side effect of the drugs, furthermore, the stability thereof is good, therefore, the preparation of the invention is a safe and effective sustained-release preparation for oral administration.
WO2009070957A1 Inhibitor of the interaction between blys and ngr and use thereof Provided are inhibitor of the interaction between BLyS and NgR and use of the inhibitor for manufacturing of a medicament for promoting neurite-outgrowth. The inhibitor can be selected from the group consisting of polypeptide, protein, small molecular compound, double stranded RNA, small RNA and RNA aptamer, preferably, the inhibitor is the polypeptide having the amino acid sequence shown in SEQ ID NO: 1. Also provided is a method of screening the inhibitor of the interaction between BLyS and NgR by use of alkaline phosphatase system (AP-system).
CN103120667A Application of Aphanamixoid A in medicine for preventing and treating renal insufficiency The invention discloses an application of Aphanamixoid A in preparation of a medicine for preventing and/or treating renal insufficiency, and belongs to the technical field of new application of the medicine. The application of the Aphanamixoid A in preparation of the medicine for preventing and treating the renal insufficiency is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on the renal insufficiency is inconceivably high; and the Aphanamixoid A has outstanding substantiality characteristic without possibility of any inspiration given by other compounds and obviously achieves the outstanding progress by being used for preventing and treating the renal insufficiency.
US20110245190 Method for improving post surgery visual acuity outcome with azithromycin The present invention relates to a method for treating dry eye disease, comprising the steps of identifying a subject suffering from dry eye disease, and administering to the subject an effective amount of azithromycin. The present invention also relates to a method for reducing contact lens intolerance in a subject, comprising the steps of: identifying a subject suffering from contact lens intolerance due to dry eye disease; and administering to the eyes of the subject an aqueous ophthalmic solution comprising azithromycin. The present invention also relates to a method for improving post surgery visual acuity outcome in a patient, comprising the steps of: identifying a patient in need of an ophthalmic surgical procedure, administering to the patient an effective amount of azithromycin prior to the ophthalmic surgical procedure, and performing the ophthalmic surgical procedures on the patient.
CN1875933A Sustained release anticancer agent carrying angiogenesis inhibitor and cytotoxic drug Disclosed is an anticancer slow release injection carrying both anti-angiogenesis agent and cytotoxic drugs, which comprises slow release micro-balloons and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents being the combination of anti-angiogenesis agent selected from Marimastat, SU5416, SU6688, Fumagillin or TNP-470, with cytotoxic drugs selected from Eptaplatin, Nedaplatin, Melphalan, 4-hydroperoxycyclophosphamide, hydroxyl radical Paclitaxel, 10-desacetyltaxuyunnanin, 7-epi-taxol, Vinorelbine, Tamoxifen, Amethopterin, Adriamycin, pidorubicin, actinomycin D, Tallimustine, Atrimustine, Semustine or Ranimustine, the slow release auxiliary materials are selected from di-aliphatic acid and sebacylic acid copolymer, ethylene-vinylacetate copolymer or lactic acid polymer, the viscosity of the suspension adjuvant is 100-3000cp and is selected from sodium carboxymethylcellulose.
US20100086494 Skin treatments containing carboxylic acid-substituted idebenone derivatives and methods of preparation and use thereof The present invention relates to novel carboxylic acid-substituted idebenone derivatives, skin treatment compositions containing these carboxylic acid-substituted idebenone derivatives, methods of treating skin changes by topical application of these carboxylic acid-substituted idebenone derivatives, and their methods of synthesis. The carboxylic acid-substituted idebenone derivatives of the present invention are unexpectedly effective in treating skin, particularly with respect to skin tolerance. When included in a topical composition, the carboxylic acid-substituted idebenone derivatives of the present invention have an antioxidant effect that is useful in treating a skin change.
WO2007009485A1 Substituted 8-phenoxy-y-carboline derivatives with 5ht1 activity The present invention provides compound of the Formula (I): and pharmaceutically compositions comprising same.
WO2011113361A1 Ceftizoxime sodium crystalline hydrate, preparation methods and uses thereof Disclosed are a ceftizoxime sodium crystalline hydrate, preparation methods and uses thereof. The ceftizoxime sodium crystalline hydrate has high storage stability, and is suitable for preparing medicaments for treating or preventing diseases of infections of respiratory system, hepatobiliary system, the five sense organs, urinary tracts, and intra-abdominal infection, pelvic infection, ichorrhemia, infection of skin soft tissues, and infection of bones and joint of human or animals bodies caused by gram positive or negative bacterias, meningitis caused by streptococcus pneumonia or haemophilus influenza, and simple gonorrhea and the like.
WO2008131936A2 Highly stable electrolytic water with reduced nmr half line width Electrolytic acid or alkaline water having a NMR half line width using 17O of from about 45 to less than 51 Hz, and an oxide reduction potential of from -1000 to +200 mV, or from +600 to +1300 mV, topical compositions that contain such water, uses for such water to hydrate skin, deliver drugs and treat various skin and mucosal conditions, and methods and apparatus for manufacturing the water.
US7514455 Derivatives of 2-pyridinol or its tautomer 2-pyridone; microorganism comprising Penicillium sp. FO-125 FERM BP-8048; antifungal antibiotics An electron transport system complex II inhibitor comprising 2-pyridinol derivative represented by the general formula [I] wherein R is alkyl or alkenyl optionally having substituent containing halogen, or its tautomer 2-pyridone derivative represented by the general formula [II] wherein R is alkyl or alkenyl optionally having substituent containing halogen, or salt thereof as an active ingredient. The compound inhibits the complex II strongly with nM order activity. Consequently, 2-pyridinol derivative or its tautomer, 2-pyridone derivative, are useful as the complex II inhibitor.
WO2008017852A1 Diamine-containing, tetra- substituted piperazine compounds as melanocortin receptor modulators There is provided compounds having the formula of structure (I): wherein the groups -C(R8)(CH2)vCH(R9)(CH2)y-Q and -C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.
CN101952260A 4, 5-dihydro-oxazol-2-yl amine derivatives The present invention relates to a compounds of formula I or a pharmaceutically active acid addition salts thereof. It has been found that the present compounds have Asp2 (ss-sccretasc, BACE 1 or Mcmapsin-2) inhibitory activity and that the compounds may therefore be used in the treatment of diseases characterized by elevated ss-amyloid levels or ss-amyloid deposits, particularly Alzheimer's disease.
US20090042843 Inhalation Device Containing Plural Doses of a Pharmaceutical Composition The invention relates to an inhalation device comprising plural of doses of a pharmaceutical composition in powder form, wherein the pharmaceutical composition comprises one or more, preferably one, anticholinergic, optionally in combination with a pharmaceutically acceptable excipient.
CN101812028A 5-chlorol-2-hydroxyl-3-(4-substituted-1H-1,2,3-triazole) benzoic acid compound as well as preparation method and application thereof The invention relates to a 5-chlorol-2-hydroxyl-3-(4-substituted-1H-1,2,3-triazole) benzoic acid compound expressed in the formula (I) as well as a preparation method and application thereof. The definition of R is shown as the specification. In the preparation method, 5-chlorolsalicylic acid used as a raw material is nitrified and reduced, is subjected to azidation and reacts with end alkyne to obtain the corresponding 5-chlorol-2-hydroxyl-3-(4-substituted-1H-1,2,3-triazole) benzoic acid compound. The compound has the inhibiting function on HIV-1 integrase, and the IC50 of part of the compound reaches 1.6 mircograms/mL, therefore, the compound is a stronger HIV-1 integrase inhibiting agent and is expected to be developed into a new HIV virus resistant medicament.
CN102008725B Application of human UTP14a expression inhibitor in preparation of cell proliferation inhibitor The invention discloses application of a human U three protein 14a (UTP14a) expression inhibitor to the preparation of a cell proliferation inhibitor. A p53 protein causes cell cycle arrest, repair after deoxyribonucleic acid (DNA) damage, cell apoptosis and the like by activating or inhibiting the expression of a downstream gene. The expression down regulating of human UTP14a can cause the rise of the p53 protein level, namely the human UTP14a expression inhibitor can promote the rise of the p53 protein level in cells so as to inhibit cell proliferation. The human UTP14a expression inhibitorcontributes to the research of the cell proliferation and the cell apoptosis, and has profound influence on the development of anti-cancer medicines.
WO2012081665A1 Substance capable of inhibiting glycine transporter The present invention relates to a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof. This compound is useful for the prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, a specific phobia, acute stress disorder, and the like), depression, drug dependence, convulsion, tremor, pain, Parkinson's disease, attention deficit/hyperactivity disorder, bipolar disorder, eating disorder, sleep disorder and the like, of which the action relies on an inhibitory activity on the intake of glycine.
CN103623021A Red ginseng extract as well as preparation method and application thereof The invention discloses a red ginseng extract. The extract is characterized by containing ginsenoside Rg1, ginsenoside Re, ginsenoside Rf, notoginsenoside R2 and ginsenoside Ro. A preparation method of the extract comprises the following steps: cutting red ginseng serving as a medicinal material into pieces, adding water in an amount which is 3-10 times that of the red ginseng, soaking for 0.5-2 hours, heating and performing reflux extraction for 1-2 hours, extracting for 1-3 times, combining extraction solutions, filtering and concentrating; separating and purifying a concentrated solution with a reverse phase silica gel column; eluting with 30-40 percent methanol-water by 4-10L, and discarding; and eluting with 50-70 percent methanol-water by 4-6L, collecting an eluent and concentrating to obtain active ingredients.
WO2011041590A2 1-desoxy-2-methylene-19-nor-vitamin d analogs and their uses This invention discloses l-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25 -hydroxy- l-desoxy-2-methylene-19-nor- vitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
US8268618 Repressing endogenous CCR5 gene expression in cells using engineered zinc finger proteins The present invention provides methods for modulating expression of endogenous cellular genes using recombinant zinc finger proteins.
WO2014084778A1 Pyrimidine-2,4-diamine derivatives for treatment of cancer A compound of formula (I), or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1.
EP1387681B1 Use of castanospermine derivatives for the treatment of hepatitis c Use of certain castanospermine esters in the treatment of diseases caused by flaviviruses, in particular in the treatment of disease caused by the hepatitis C virus (HCV) and compositions containing said esters in combination with adjunctive therapeutic agents.
CN1736262A Composition containing flavonoid, jphosphatidyl inositol and/or inosite Disclosed is a composition containing flavonoid substance, phosphoinositide and/or inositol, characterized in that the mass parts of the ingredients include, flavonoid substance 0.001-10000.0 parts, phosphoinositide and/or inositol 0.001-10000.0 parts. The composition can be used for the prevention and treatment of atherosclerosis and diabetes.
US7563822 active ingredient a 5-amidino-2-hydroxybenzenesulfonamide derivative or a pharmaceutical acceptable salt thereof; excellent inhibitory effect on mesangial cell proliferation and decreasing effect on urine protein excretion The present invention relates to an agent for the prevention or treatment of a renal disease comprising as an active ingredient a 5-amidino-2- hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted alkyl group; R2 is a dialkylamino group, an alkyl group, a cycloalkyl group, an optionally substituted aryl group etc.; T is an oxygen atom, a sulfur atom etc.; Q is a hydrogen atom or an optionally substituted alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof which has an inhibitory effect on mesangial cell proliferation and a decreasing effect on protein excretion in urine, and are useful for preventing or treating of various renal diseases such as IgA nephropathy, diabetic nephropathy, nephritic syndrome and the like.
US20110021621 Drug for treating circulatory insufficiency The present invention relate to a drug for treating circulatory insufficiency containing a benzopyran derivative represented by the following general formula (I): and/or a physiologically acceptable salt thereof as an active ingredient, wherein R1 is an alkyl group having 1 to 10 carbon atoms, or an alkenyl group having 2 to 10 carbon atoms; and any one of R2, R3, R4 and R5 is a hydroxyl group, an alkoxy group, an alkenyloxy group, an alkoxy group substituted with a hydroxyl group, or an alkoxy group substituted with a carboxy group, and the others are hydrogen atoms.
US20130030024 Method of Administering Pirfenidone Therapy The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes.
US20110300186 Functionalized Nano- and Micro-materials for Medical Therapies Compositions containing an optionally surface-functionalized mesoporous support and a biologically active agent, and pharmaceutical compositions of the same, are provided herein. Such compositions can be useful in the treatment of tumors, for example, by injection of the composition at a location near the site of the tumor.
CA2601795A1 Chewing gum compositions of varenicline A chewing gum composition including a water insoluble base portion; a water soluble portion; and a therapeutically effective amount of varenicline or its pharmaceutical acceptable salt thereof. A method for reducing nicotine addiction and aiding in the cessation or lessening of tobacco use in an individual by administering to an oral cavity of an individual a chewing gum composition including an effective amount of varenicline or its pharmaceutical acceptable salt thereof; and chewing the gum composition to cause the varenicline or its pharmaceutical acceptable salt thereof to be released from the chewing gum composition into the oral cavity of the individual. A method of manufacturing a chewing gum composition.
CN102885847A Novel uses of camellia oleifera cake polysaccharide The invention relates to novel uses of plant extract and especially relates to novel uses of camellia oleifera cake polysaccharide. The invention provides the use of camellia oleifera cake polysaccharide in inhibition of alpha-glucosidase activity and also provides the use of camellia oleifera cake polysaccharide in preparation of a drug for treating diabetes.
US7015230 serine protease inhibitors comprising pyrimidinediones, used as anticoagulants for prophylaxis of cardiovascular disorders; thrombolytic agents The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
WO2011066352A1 An amorphous and a crystalline form of genz 112638 hemitartrat as inhibitor of glucosylceramide synthase The hemitartrate salt of a compound represented by the following structural formula: (Formula I Hemitartrate), which may be used in pharmaceutical applications, are disclosed. Particular single crystalline forms of the Formula (I) Hemitartrate are characterized by a variety of properties and physical measurements. As well, methods of producing crystalline Formula (I) Hemitartrate, and using it to inhibit glucosylceramide synthase or lowering glycosphingolipid concentrations in subjects to treat a number of diseases, are also discussed. Pharmaceutical compositions are also described.
CN102176918A Treating or preventing gout Use of glycomacropeptide to treat or prevent gout, use of one or more phospholipids and one or more gangliosides to treat or prevent gout, or use of glycomacropeptide and one or more phospholipids and one or more gangliosides to treat or prevent gout.
US20110152361 Novel epigallocatechin gallate tetramer and vascular endothelial function improving agent containing the same Providing a compound capable of continuously taking and having a vascular endothelial function improving effect by enhancing NO function from the vascular endothelial cells. A compound represented by Formula (I) wherein R1, R2, R3 and R4 are each independently H or a gallate group, a vascular endothelial function improving agent, food and drink or pharmaceutical composition containing the compound.
WO2013028818A1 Pyrimido- pyridazinone compounds and use thereof The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
US20110117194 Pharmaceutical formulation containing angiotensin-ii receptor blocker The present invention provides a pharmaceutical formulation containing an angiotensin-II receptor blocker and a release-control material as a pharmacologically active ingredient and a pharmaceutical formulation comprising an immediate-release compartment and an extended-release compartment. The immediate-release compartment contains an agent as a pharmacologically active ingredient for preventing and inhibiting hepatitis and the extended-release compartment has an angiotensin-II receptor blocker as a pharmacologically active ingredient. The formulation of the present invention maximizes the effectiveness on pharmacologically and clinically lowering blood pressure and preventing complications when taking the formulation, helps to avoid interaction with a drug which is metabolized by the same enzyme in the liver, and prevents and inhibits the incidence of drug-induced hepatitis which is caused by drug administration for a long time.
CN103652939A Capsule with multiple vitamins C The invention provides a capsule with multiple vitamins C for supplementing daily nutrient for a human body. According to the capsule, three or more of ferrous vitamin C, vitamin C calcium, vitamin C sodium, vitamin C and vitamin C derivatives are taken as the main raw materials and are crushed, sieved and mixed to prepare the capsule. As the performance of the capsule with multiple vitamins C is stable, the solubility of the contents in water is good, the absorptivity of a human body is high, the pH value ranges from 7.2 to 7.8 and the safety performance is good; vitamin C, vitamin ferrum and vitamin calcium are supplemented at the same time, and the capsule can substitute for a conventional single or compound vitamin C-type oral preparation. The capsule with multiple vitamins C is to become a new consumption hotspot of vitamin C-type supplements.
CN101683339A Drug composite containing lansoprazole and naproxen The invention relates to a drug composite containing lansoprazole and naproxen, which takes lansoprazole and naproxen as active constituents and forms the drug composite by mixing acceptable accessories pharmaceutically; in the composite, the weight ratio of the lansoprazole and naproxen is 1;3-1:33, 1:17 is preference. The drug composite can be prepared into oral preparation and is used for treating rheumatoid arthritis, osteoarthritis and ankylosing spondylitis patients who use non-steroidal anti-inflammatory drugs to cause gastrohelcosis danger possibly.
WO2013139727A1 Triazines with suitable spacers for treatment and/or prevention of hiv infections The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.
CN101417126A New use of OMI protein and coding gene thereof The invention discloses a new usage of an OMI protein and a coding gene thereof. The new usage provided by the invention relates to the application of the OMI protein and the coding gene thereof in preparing a medicament which can promote the degradation of the protein of an A53T Alpha-synuclein mutant, the application in preparing a medicament for curing parkinsonism, the application of promoting the degradation of a lysoome and the application of preparing a medicament for promoting the degradation of the lysoome. The OMI protein is a protein which is formed by an amino acid sequence demonstrated by the sequence 4 in a sequence list; and the coding gene of the OMI protein is a DNA molecule demonstrated by the sequence 3 in the sequence list. The invention links the OMI protein and the coding gene thereof with the degradation activity of the lysoome, discloses the adjusting function of the protein on a cell acid organelle-lysoome and the promoting effect on the degradation of A53T Alpha-synuclein-EGFP protein, provides a new concept for the clinic curing of the parkinsonism and has great significance.
CA2458001C Regulation of immune responses by manipulation of intermediary metabolite levels The present invention provides novel processes for regulating immune responses in mammalian subjects, e.g., humans, afflicted with diseases such as cancers, infections, e.g., viral infections, bacterial infections, or immune dysfunctions, especially auto-immune disorders, e.g., diabetes, Crohn's disease, rheumatoid arthritis, arteriosclerosis and ulcerative colitis. More particularly, this invention relates to generating elevated levels of an intermediary metabolite, e.g., lipids or conjugated biomolecules, e.g., glycolipids, lipoproteins and glycoproteins other than antibodies, cytokines or hormones. Treatment can be carried by introduction of the intermediary metabolite into the afflicted subject or by a reagent that when administered leads to elevated levels. The treatment regimen can be in vivo or ex vivo.
CN102836134A Method for preparing mesylate arbidol freeze-dried powder injection preparation A method for preparing a mesylate arbidol freeze-dried powder injection preparation, which comprises the step of adding mesylate arbidol and mannitol into water for injection, wherein the pH (Potential Of Hydrogen) value of the water for injection is 2.5 to 3.5. Due to the acidic environment provided by the invention, mesylate arbidol is easy to dissolve and can not separate out crystals, a phenolic hydroxyl group in a molecular structure is relevantly stable and not subjected to oxidative denaturation under the acidic environment, and the heat source removing operation is avoided under the high temperature of 60 to 70 DEG.C. The content of mesylate arbidol of the obtained preparation can reach up to above 99%, the content of the maximum impurities is only 0.16%, the number of the impurities is 3 and the total content of the impurities is only 0.38%. However, the total content of the impurities in the preparation in the prior art is up to 0.67%.
US8759369 Inhalable solid amorphous particles comprising tiotropium bromide and a co-solid An inhalable medicament is provided, in particular a new solid-state form of tiotropium bromide. The medicament can be in the form of solid amorphous particles containing an intimate admixture of tiotropium bromide together with a pharmaceutically acceptable co-solid having a glass transition temperature of at least −50° C., such as a sugar and/or sugar alcohol.
CN1981754A Silybum dropping balls and their production A dripping pill of silibinin is prepared from silibinin and matrix in weight ratio of 1: (4-12) through fusing and dripping.
US20110076283 Method for predicting and diagnosing brain tumor The present invention relates to a method for predicting or diagnosing outcome of concomitant chemo-radiotherapy of a subject suffering from brain tumor. The present invention further relates to compositions and methods for treatment or prevention of tumor resistance in a subject suffering from a brain tumor and to a kit useful for predicting or diagnosing the tumor resistance in a subject treated with concomitant chemo-radiotherapy.
CN1970007A Capsule for improving sexual function for men Disclosed is a capsule for improving sex functions which is prepared from yohimbine, ginkgo extract, gen-seng extract, epimedium extract, wolferry fruit extract, arginine, zinc gluconate, nicotinic acid, lycopersicin, vitamin A, vitamin E and vitamin C.
CN102796124A Di-beta-carboline alkali compound and preparation method, medicinal composition and application thereof The invention discloses a di-beta-carboline alkali compound and a preparation method, a medicinal composition and application thereof. The di-beta-carboline alkali compound and pharmaceutical salt thereof are shown as a general formula I. The di-beta-carboline alkali compound is prepared by condensing a beta-carboline intermediate and dihalogenated alkane. The medicinal composition comprises an effective dose of di-beta-carboline alkali compound shown as the formula I and a pharmacodynamically acceptable carrier. The invention also discloses application of the di-beta-carboline alkali compound to preparation of medicines for resisting tumors such as melanoma, gastric cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermal carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostatic cancer and colon cancer.
US20120064121 Pyridine compounds for inflammation and immune-related uses The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
US7256310 L-tartrate derivative; stable particle size distribution; reproducible dosing; can be stored under varying temperature and humidity conditions Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.
CN1978447A 10-hydroxy camptothecin arginine salt, and its preparing method and use This invention relates to 10-hydroxycamptothecin arginine salt like the structure of formula (I). The preparation of this compound is in condition of water participating. 10-hydroxycamptothecin lactone is unfolded, of which carboxy group first bonds with amino-group of arginine to produce salt, then bonds with 10-phenolic hydroxyl group, then bonds with other arginine acid by hydrogen bond pattern. The quantity of adding arginine can be from 1 to 8 times of molar ratio. The water solubility of 10-hydroxycamptothecin arginine salt and its association object is obviously better than 10-hydroxycamptothecin. It overcomes flaws such as noxious property of camptothecin sodium is high, stability is bad. It provides a medicine of which curative effect is reliable, medication is safe and cost is low for tumor patient.
US20080132472 Compounds for the treatment of psychiatric or substance abuse disorders The invention provides methods for treating or preventing psychiatric and substance abuse disorders, involving administration of a therapeutically-effective amount of a cytosine-containing or cytidine-containing compound, creatine-containing compound, adenosine-containing, or adenosine-elevating compound to a mammal.
EP2701704A2 Methods of administering anatabine to treat autism spectrum disorders and seizure disorders Pharmaceutical compositions comprising a compound of Formula I, e.g., an isolated form of anatabine or S-(-)-anatabine, or a pharmaceutically acceptable salt thereof, can be used to treat Autism Spectrum Disorders and seizure disorders.
CN102743756A Compound preparation of propiverine hydrochloride and alpha-receptor antagonist The invention discloses a compound preparation of propiverine hydrochloride and alpha-receptor antagonist and application thereof, belonging to drug field. The compound preparation includes, in unit preparation, 5-40 mg of propiverine hydrochloride and 0.1-10 mg of alpha-receptor antagonist. The compound preparation comprises propiverine hydrochloride and alpha-receptor antagonist as main drug and can treat overactive bladder (OAB) complicated with benign prostate obstruction (BPO), significantly improve patient living quality and improve patient compliance of drug treatment; and has good clinical application prospect.
CN101374532A Use of gallium to treat biofilm-associated infectons The invention provides methods, compositions, and kits for treatment or prevention of biofilm-associated infections in an individual. Methods of the invention include administration of a gallium-containing composition for treatment of an established biofilm or prevention of formation of a biofilm. Some methods include administration of a gallium-containing composition in conjunction with an antibiotic substance. Some methods include treatment or prevention of an orally-associated biofilm with a gallium-containing composition in the form of a dentrifice, mouthwash, or chewing gum composition.
US20080085877 Therapeutic methods of using estrogen compositions A method for preventing or treating a catamenial migrainous disorder in a female subject comprises administering to a vulvovaginal surface of the subject a pharmaceutical composition that is bioadhesive thereto and comprises at least one estrogenic compound in an amount of about 50 μg to about 1000 μg estradiol equivalent per unit dose of the composition. A related method comprises administering to a vulvovaginal surface of the subject a pharmaceutical composition comprising at least one estrogenic compound, wherein upon administration of the composition to the vulvovaginal surface, a decline in serum estradiol concentration during a luteal phase of a menstrual cycle is moderated.
WO2014061031A1 2-phenyl-5-heterocyclyl-tetrahydro-2h-pyran-3-amine compounds for use in the treatment of diabetes and its associated disorders The present invention relates to novel compounds of the general formula (I) their tautomeric forms, their enantiomers, their diastereoisomers, their pharmaceutically accepted salts, or pro-drugs thereof, which are useful for the treatment or prevention of diabetes mellitus (DM), obesity and other metabolic disorders. The invention also relates to process for the manufacture of said compounds, and pharmaceutical compositions containing them and their use.
CN102793707A Novel purpose of N-acetylglucosamine The invention relates to a novel purpose of N-acetylglucosamine, which is capable of treating arthritis deformans and promoting cartilage repair. By long-term research and repeated tests, the inventor founds and proves that the N-acetylglucosamine has the novel purpose besides cosmetic, the N-acetylglucosamine can be effectively used for treating arthritis deformans and promoting cartilage repair, and the usage is convenient.
EP1361885B1 Use of gamma-gt inhibitors for the treatment of chronic degenerative diseases Use of η-GT inhibitors for the preparation of a pharmaceutical composition for the treatment of a degenerative disease, in particular of chronic renal diseases or inner ear degenerative diseases.
CN101810720A Skin disease external powder for comprehensively killing and inhibiting bacteria and diminishing inflammation and using method thereof to beriberi skin disease The invention discloses a skin disease external powder for comprehensively killing and inhibiting bacteria and diminishing inflammation, which comprises the following raw materials in part by weight: 10 to 100 parts of talcpowder, 1 to 20 parts of metronidazole, 1 to 10 parts of phellodendron, 1 to 10 parts of borneol, 1 to 10 parts of menthol, 1 to 10 parts of griseofulvin, 1 to 5 parts of chloramphenicol, 1 to 5 parts of sulfamethoxazole, 1 to 5 parts of aspirin, 1 to 5 parts of alum, 1 to 3 parts of chlortrimeton and 1 to 3 parts of vitamin B1. The invention also relates to a using method of the skin disease external powder for comprehensively killing and inhibiting bacteria and diminishing inflammation to beriberi skin disease. The medicaments are effectively combined, and the effects of the medicaments are supported one another, so the skin disease external powder has the effects of comprehensively killing poison, killing and inhibiting bacteria, diminishing inflammation, relieving itching, killing pain, clearing away heat, releasing toxin, restraining sweat gland, removing sweat and deodorizing on an affected part, and simultaneously has effects of killing and inhibiting bacteria and disinfecting on the environment of the affected part so as to fulfill the aims of radically curing fungi and bacterial infection skin disease and restoring the skin.
CN102061280A Bacillus subtilis SWB8 for producing diosgenin The invention discloses a Bacillus subtilis WB8 capable of producing diosgenin, and belongs to the technical field of applied microbiology. The strain is separated from internal issues of subterraneous stems of a medicinal plant of Dioscorea zingiberensis wright, can synthesize and secrete a metabolin of a host plant, namely diosgenin, and has the preservation number of CCTCC (China Center For Type Culture Collection) NO:M2010271; and the strain is rod-like, has the size of 1-1.5*3-5 mu m, forms a single-chain sporocarp, releases endospore, has rough colony with grid bulges, forms pellicle through liquid fermentation, has rich foam, and can grow 16SrDNA core sequence 1542bp with the thermophilic temperature of between 30 and 35 DEG C, the pH of 6.0-9.0 and capacity of tolerating 9.0 percent NaCl, wherein the core sequence has the sequence number of HM210636. The strain liquid is fermented by a common culture medium for 48 to 60 hours, the chloroform extract of the fermentation liquor is the diosgenin, and the diosgenin has the activity of inhibiting pathogenic bacteria and resisting tumor cells. The strain provided by the invention can produce the diosgenin; and compared with the conventional process of extracting the diosgenin from yam plants, the method avoids the pollution of strong acid and yam byproducts on environment, and has potential industrial application prospect.
WO2008148292A1 An ophthalmic, otic or nasal composition and its use An ophthalmic, otic or nasal composition comprises levofloxacin or pharmaceutical salts thereof and loteprednol etabonate, wherein the weight ratio of loteprednol etabonate to levofloxacin is 1 : 0.2-5. The ophthalmic, otic or nasal composition of the invention is useful for treating conjunctivitis, keratitis, blepharitis, dacyrocystitis, hordeolum and corneal ulcers and ocular infection accompanied by ocular, even its peripheral tissue inflammation, or preventing the bacteria infection and furthermore the tissue inflammation of the infected part after the ophthalmic operation or ocular injury, or treating or relieving the bacteria infectionin combination with the tissue inflammation of the infected part, or treating tympanitis, meatus acustici externi isthmus and infective rhinitis.
US20090304823 Nutritional compositions for promotion of bone growth and maintenance of bone health and methods regarding same Compositions and methods for maintenance of bone health or prevention, alleviation and/or treatment of bone disorders are presented. The present invention also provides the manufacture of a nutritional product, a supplement or a medicament for promoting bone growth or for the maintenance of bone health and methods regarding same. In an embodiment, the present invention provides a composition comprising an active ingredient having an effective amount of a plant or plant extract containing at least one phytochemical having the ability to induce bone morphogenic protein expression.
US7056939 4-(4Methoxybenzyl)-n′-(5-nitro1,3-thiazol-2-yl)urea and its use in the treatment of conditions associated with glycogen-synthase kinase-3 (gsk3) The present invention relates to a new compound of formula I as a free base or a pharmaceutically acceptable salt thereof, a process for the preparation, pharmaceutical formulations containing said therapeutically active compound and to the use of said compound in therapy.
CN100999500A Onitrodazole precursor drug and its preparation process and use This invention involves Ornidazole precursor drug and its preparation and use. Ornidazole precursor drugs is obtained by through chemical modification to its structure of the hydroxyl group, can be used in medicinal combination, can be used to treat anaerobic bacteria or protozoan infection diseases.
CN101368180A Small RNA numerator for differentiation of mesenchyma stem cell into hematopoiesis cell and function target point thereof The invention provides small RNA (shR337) capable of differentiating hematopoietic stem cells (MSC) from human nonhematopoietic stem cells (HSC) such as mesenchymal stem cells (MSC). The discovery of the small RNA also provides an action target capable of differentiating the hematopoietic stem cells from the human nonhematopoietic stem cells such as the bone marrow mesenchymal stem cells. The small RNA can restrict the protein translation of EIDI genes after being transfected to human bone marrow mesenchymal stem cells to transform the human bone marrow mesenchymal stem cells into hematopoietic stem cells with CD45<+>surface antigen positive, and the hematopoietic stem cells with CD45<+>surface antigen positive can be further differentiated into myeloid cells and lymphoid cells. Mice in vivo experiments show that the differentiation of the small RNA to the mesenchymal stem cells is directional and undivided.
US7553868 2-[(Aminocarbonyl)amino]-5-[2-{2-[{N-(2-chlorobenzyl)-N-methyl}amino]ethoxy}phenyl]-thiophene-3-carboxamide; serine/threonine kinase inhibitors; antiinflammatory agents; asthma; rheumatic diseases; antiarthritic agents; multiple sclerosis; chronic obstructive pulmonary disease The invention relates to thiophene carboxamides of formula (I) wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
CN1775210A Ftibamzone eyedrops The present invention relates to a kind of ftibamzone eye drops. It contains the components of ftibamzone, osmotic pressure regulating agent, preservative, Tween 80, thickening agent, EDTA and sodium hydroxide.
WO2012147890A1 Novel azole derivative The present invention relates to a nitrogen-containing aromatic compound according to formula (I) that acts as an effective inhibitor of phosphodiesterase 10 (PDE 10). The present invention also relates to a pharmaceutical composition containing this type of compound, and the use of this type of compound in methods for treating certain types of central nervous system (CNS) disorders and other disorders. The present invention also relates to a method for treating disorders such as a neurodegenerative disorders and mental disorders such as schizophrenia disorders, as well as disorders that include cognitive disability as a symptom.
CN1634099A Swerianmarin injectio, its preparation process and application The invention discloses a Swerianmarin injection, its preparation process and application, wherein the preparing process comprises using Gentianaceae, Scrophulariaceae or Oleaceae plants as raw material, employing conventional phytochemical method for extraction, segregation and purification, thus obtaining swertiamarin, weighing swertiamarin and medicinal adjuvant, charging water for injection, thermal insulating 10-20 minutes at 30-60 deg. C, cooling down, filtering, dispensing the filter liquor 1-48 hours at 0-5 deg. C, filtering, encapsulating, drying in frozen, sterilizing, and packaging.
EP1838313A2 Pharmaceutical composition comprising nifedipine and mesalazine for the treatment of rectoanal tenesmus A pharmaceutical composition is disclosed including nifedipine and mesalazine that can be used for the treatment of rectoanal tenesmus.
EP2086964A2 Benzoyl amino heterocyclyl compounds useful in the treatment of a disease mediated through glk The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).
US20080220001 Using heterocyclic sulfonamide specific to carbonic anhydrase as therapeutic tools in treatment of tumor disorders Therapeutic methods for inhibiting the growth of preneoplastic/neoplastic vertebrate cells that abnormally express MN protein are disclosed. Screening assays are provided for identifying compounds, preferably organic compounds, preferably aromatic and heterocylic sulfonamides, which inhibit the enzymatic activity of MN/CA IX and that are useful for treating patients with preneoplastic/neoplastic disease. Further, the CA IX-specific inhibitors when labeled or linked to an appropriate visualizing means can also be used diagnostically/prognostically for preneoplastic/neoplastic disease, and for imaging use, for example, to detect hypoxic precancerous cells, tumors and/or metastases, by selectively binding to activated CA IX, preferably CA IX activated under hypoxic conditions, and not to inactive CA IX. Such detection of hypoxic conditions can be helpful in determining effective treatment options, and in predicting treatment outcome and the prognosis of disease development. Still further, the CA IX-specific inhibitors can be used therapeutically to selectively target hypoxic cells expressing activated CA IX. The CA IX-specific inhibitors can be labelled or conjugated to radioisotopes for radiotherapy of hypoxic cells. Alternatively, the CA IX-specific inhibitors can be used for gene therapy coupled to vectors for targeted delivery to hypoxic preneoplastic/neoplastic cells expressing activated CA IX on their surfaces. In an alternative mode of the invention, CA IX-specific inhibitors may be used therapeutically to target acidic conditions of a tumor, e.g., to increase pHe in order to enhance the efficacy of weak base chemotherapeutic drugs.
CN101317882A Common cold-proof tea particle for children The present invention relates to an anti-cold tea granule for children, which is characterized in that honeysuckle, chrysanthemum, ageratum, mint, Chinese thorowax root and Chinese radish seed are extracted for obtaining concentrated solution to be made into extract powder and VC which are mixed together and stirred uniformly, then the mixture is granulated, dried and sterilized to obtain the anti-cold tea granule for children.
US20130183318 Methods and compositions for the inhibition of stat5 in prostate cancer cells The present invention relates to compositions and methods for the treatment of prostate cancer. In certain embodiments, the invention relates to compositions and methods for the inhibition of prostate cancer cell growth, comprising inhibiting the activity of Stat5 in prostate cancer cells.
WO2006043518A1 Drug for treating neurological disease Disclosed is an urea compound having a structure represented by the general formula [1] below which has a new pharmacological effect. The urea compound having the structure represented by the general formula [1] below or a salt thereof has an excellent curative effect on neurological diseases. In the formula below, A represents -(NR4)-, -(CR5R6)- or -O-; B represents an alkylene or alkenylene group; R1, R2, R4, R5 and R6 respectively represent a hydrogen atom, an alkyl group, an alkenyl group, an adamantylalkyl group or the like; R3 represents an aryl group or an unsaturated heterocyclic ring; and X represents an oxygen atom or a sulfur atom.
CN103690857A Herbal medicine footbath powder for treating rheumatism The invention discloses herbal medicine footbath powder for treating rheumatism. The grass medicine footbath powder comprises 15 percent of sargentodoxa cuneata, 15 percent of ventilago leiocarpa benth, 10 percent of pterospermum heterophyllum, 8 percent of climbing entada, 8 percent of daphniphyllurn calycinum benth, 26 percent of alpinia japonica, 13 percent of aquilaria sinensis and 5 percent of health care magnet. The herbal medicine footbath powder has a certain treatment function, and has the effect of treating rheumatism and numbness of limbs.
CN103012187A Novel diacetyl acetic acid quadrol compound and drug combination thereof The invention discloses a novel diacetyl acetic acid quadrol compound which is obtained through recrystallization for many times, wherein the purity of the compound is larger than 99.6 percent. The invention also discloses a drug combination of the diacetyl acetic acid quadrol compound, which comprises the following compositions in parts by weight: 200-600 parts of diacetyl acetic acid quadrol, 10-30 parts of sophocarpidine, 3-8 parts of sorbitol, 1-6 parts of sodium bicarbonate and 2-10 parts of malic acid. According to the drug combination disclosed by the invention, the sophocarpidine is matched with the diacetyl acetic acid quadrol, thus greatly improving the hemostatic effect of the diacetyl acetic acid quadrol and also lowering the probability of adverse reaction; and synergistic effect is generated among the sorbitol, the sodium bicarbonate and the malic acid, thus greatly improving the stability of the diacetyl acetic acid quadrol under the conditions of high temperature, high humidity and high lights.
US20100154072 siRNA Kinase and Methods of Use The invention is based on the finding that Clp1 has the activity of an RNA kinase. Clp1 is therefore useful as an enhancer of siRNA activity. It can be used per se, in kits or expressed in cell lines. Clp1 transgenic and Clp1 knock-out non-human animals are useful for studying the function of siRNAs. Clp1 is also useful in gene therapy to enhance the efficacy of therapeutic siRNAs.
EP0971585B1 Tetracycline compounds in the treatment of certain types of cancers The invention is a method of inhibiting cancer growth, by inhibiting cellular proliferation, invasiveness, or metastasis, or by inducing cytotoxicity against cancer in mammals. The method employs 6-demethyl-6-deoxy-4-de(dimethylamino)tetracycline (CMT-3) and other functionally related chemically modified, preferably non-antibacterial, tetracycline compounds to inhibit cancer growth. The method is particularly effective to inhibit the establishment, growth, and metastasis of solid tumors, such as tumors derived from colon cancer cells, breast cancer cells, melanoma cells, prostatic carcinoma cells, or lung cancer cells.
CN101524428A Gel paste for treating eczema, ecthyma, and impetigo The invention relates to a Juisheng san gel paste for treating eczema, ecthyma, and impetigo, which is characterized in that sodium carboxymethyl cellulose and other gels are compounded into a paste matrix; and the paste carries with carbon powder which is obtained by burning and baking a Juisheng san water suspending agent and residue thereof. The gel paste comprises the following advantages that: 1, the paste has hemostasis function; 2, the paste has the function of inhibiting the growth of bacteria; 3, the paste can prolong the time of medicament release; 4, the paste generates the bioadhension so as to firmly adhere to an afflicted part; 5, the paste has adsorption function on moisture, ulcer and ichor of the skin; 6, the paste has the functions of inhibiting the growth of fibrocyte and reducing scars; 7, the paste forms a film state on the afflicted part under the action of the temperature and under the natural condition; 8; the paste does not adhere to the skin and is easy to remove so as to not cause secondary bleeding and damage; 9, the paste makes a preparation more stable; and 10, the paste has convenient use.
CN1857232A Biodegradable nano magnetic capsule loading medicine and its preparing process The medicine carrying biodegradable nanometer magnetic capsule in core-shell structure includes a composite shell layer comprising a continuous phase of biodegradable polymer material and a dispersed phase of nanometer magnetic particle, and a core formed with water soluble or hydrophilic medicine. Its preparation process includes: dissolving medicine and surfactant or emulsifier in water to obtain the dispersed system A; mixing biodegradable polymer, nanometer magnetic particle and organic solvent to obtain dispersed system B; dispersing surfactant or emulsifier in water to obtain dispersed system C; mixing the dispersed system A, the dispersed system B and the dispersed system C; and stirring to evaporate organic solvent to obtain the required structure. The present invention has simple and controllable process, and the prepared capsule has high medicine carrying quantity, controllable release of medicine, target medicine release and capacity of being monitored.
CN103054809A Curcumin-particle-containing sustained-release microsphere with high medicament loading capacity as well as preparation method and application thereof The invention discloses a curcumin-particle-containing sustained-release microsphere with high medicament loading capacity as well as a preparation method and application thereof. Because curcumin is micronized before being used for preparing sustained-release microspheres, the prepared sustained-release microspheres have high encapsulation efficiency, high medicament loading capacity and good sustained release effect and are free from burst release, and in addition, the prepared sustained-release microspheres have stable and controllable quality, can be used clinically, safely and effectively and are suitable for industrial application.
CN100579527C Compositions comprising immunomodulatory compounds for the treatment and management of myelodysplastic syndromes and use method thereof Methods of treating, preventing and/or managing myelodysplastic syndromes are disclosed. Specific methods encompass the administration of immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active ingredient, and/or the transplantation of blood or cells. Specific second active ingredients are capable of affecting or blood cell production. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
CN102008618A Externally used plaster for treating ulcers and bone diseases and preparation method thereof The invention belongs to an externally used plaster, in particular to an externally used plaster for treating ulcers and bone diseases and a preparation method thereof. The plaster is prepared by processing effective quantity of musk, bezoar, borneol, frankincense, myrrh, rhubarb, scorpion, chilopod, dragon's blood, carbonized hair, pyrolusite, native copper, unprocessed semen strychni, minium and sesame oil. By means of the invention, the problems that the plaster in the prior art can not directly reach focus for treatment, and the medicament has slow response, long treatment cycle and the like can be solved. The plaster provided by the invention has reasonable apolegamy of raw materials and simple preparation method, can directly reach the focus of a patient in the treatment process, and has the advantages of quick response and high recovery rate. The plaster has the advantages that a surgery is no need of being carried out in the treatment process, scars are not left, the patient does not suffer from pains, and the like.
US20100056622 Methods of Using Ramelteon to Treat Patients Suffering from a Variety of Neurodegenerative Diseases Methods of using ramelteon to treat patients suffering from a variety of neurodegenerative diseases are disclosed.
WO2007110243A8 Medicament, cosmetic or food product comprising an indol compound, the use thereof and the method of isolation thereof from sauerkraut The present invention provides a medicament comprising a chemical compound according to formula A: wherein Rl is hydrogen, fluorine, chlorine, bromine, hydroxy, mercapto, methoxy, ethoxy, acetoxy, methyl, ethyl, propyl, isop- ropyl, t-butyl, nitro, amin, N,N-dimethylaminoyl, N,N-diethyl- aminoyl; R2 is hydrogen, a C1-8-alkyl e.g. methyl, ethyl, propyl, isopropyl, butyl, t-butyl; an C1-8-acyl e.g. acetyl, propionyl; R3 is a C5-12-heterocyclic ring, e. g. furanyl, pyranyl, pyrrolyl, pyridinyl, pyrazolyl, thienyl, thiazolyl, indolyl or -0R4; R4 is a C5-C12-aromatic ring e.g. phenyl; unsubstituted or substituted in any position with fluorine, chlorine, bromine, methoxy, eth oxy, C1-8-carboxy; Z is OH or 0; and n is 0, 1, 2 or 3, and m is 0, 1, 2 or 3, and its use for the activation of the aryl hydro carbon receptor.
CN102058045B Beverage for supplementing human body energy and recovering people from fatigue The invention discloses a drink for supplementing human body energy and recovering people from fatigue as well as a preparation method and application thereof. The beverage is characterized by containing glucose-6-phosphate. The preparation method comprises the following steps: mixing glucose, adenosine triphosphate (ATP) and magnesium chloride; and obtaining a mixed solution containing glucose-6-phosphate in the presence of hexokinase serving as a catalyst. Besides the glucose-6-phosphate, the beverage provided by the invention also contains a defined amount of components such as glucose, sodium ions, potassium ions, magnesium ions, and the like. The components, after being combined, can fully perform a synergistic action, and effectively perform functions of quickly supplementing human body energy, and recovering people from fatigue. Meanwhile, the beverage can supplement the potassium ions, the sodium ions and the magnesium ions, and achieve a function of maintaining acid-base balance of a human body and improving the immunity. The nutrient solution containing glucose-6-phosphate is mild, suitable for long-term consumption and free of side effects.
EP2610259A1 Free crystal of tricyclic pyrazolopyrimidine derivative To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.
CN103705475A Artesunate freeze-dried powder injection composition and preparation method thereof The invention discloses an artesunate freeze-dried powder injection composition and a preparation method thereof. The artesunate freeze-dried powder injection composition comprises the following components in parts by weight: 120 parts of artesunate, 10-20 parts of lecithin, 20-40 parts of L- lysine. The preparation method comprises the following steps of 1, dissolving the L-lysine in injection water; 2, dissolving the artesunate and the lecithin in officinal alcohol; 3, uniformly mixing the two solutions, filtering by using a microfiltration membrane of 0.2-2mu m, fixing a volume of filtrate by using the officinal alcohol, regulating pH to be 5.0 by using a NaOH solution, canning, carrying out half-plugging and freeze-drying, and plugging to obtain the artesunate freeze-dried powder injection composition. The artesunate freeze-dried powder injection composition prepared by adopting the preparation method is easy to dissolve, and good in heat stability.
CN102532211A Lignan triglycoside compound and preparation method and application thereof The invention discloses a lignan triglycoside compound and a preparation method and application thereof. The molecular formula of the lignan triglycoside compound is C38H56O22. The preparation method comprises the following steps of: placing crushed Castanea henryi (Skan) Rehd.et Wils husks into an organic solvent for extraction, separating to prepare the extract solution, extracting the extract solution, and preparing the extract via concentration of the extract solution; and carrying out chromatographic separation and purification of the extract to prepare the lignan triglycoside compound. The organic solvent is one or mixture of methanol, ethanol, butanol and acetone. The lignan triglycoside compound with the novel structure is prepared via extraction and separation of the Castanea henryi (Skan) Rehd.et Wils husk, has good antioxidant activity, can be applied in preparation of antioxidants, antioxidant drugs, antioxidant cosmetics or antioxidant health food, and has good development prospect.
CN102836262A Immunity-improving health care product The invention discloses an immunity-improving health care product, whcih is composed of the following raw materials: 20-50g of platycladi seeds, 10-30g of radix clematidis, 10-30g of willow branches, 20-50g of fructus aurantii, 10-30g of Aurantii Immaturus Fructus, 30-60g of Gardenia jasminoides Ellis, 10-30g of omphalia, 5-25g of gynura bicolor, 5-25g of Ganoderma sinensis, and 10-30g of cubilose. The health care product provided in the invention can powerfully improve human body immune cell activity, quickly destroy and eliminate bacteria, prevent pathological changes, and has an obvious effect as well as no toxic or side effect.
US20090149551 OXIDIZED cis-TERPENONE AND ITS USE AS A CHEMOPROTECTIVE AND ANTI-MALARIAL AGENT 4b,5,6,7,8,8a-cis-hexahydro-2-hydroxy-4b,8,8a-trimethylphenanthren-9,10-dione (OHCT) is a fully oxidized compound based on the 2-hydroxy-cis-terpenone (HCT). Because OHCT is fully oxidized, it is more stable and less likely to damage cells or cell constituents such as DNA. OHCT has antimalarial activity, noncompetitive inhibitory activity against carcinogenic conversion of aflotoxin B1 (AFB1) to exo-AFB1-epoxide thus inihibiting AFB1 induced cellular toxicity, and inhibitory activity against TCDD induced cellular toxicity.
US6900222 Relaxant drugs; antiulcer agents The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.
US20100008900 Annexin ii compositions for treating or monitoring inflammation or immune-mediated disorders Methods and compositions for treating, detecting, diagnosing or assisting in the diagnosis of an inflammatory or immunological disorder are provided. The authors have made the novel discovery that anti-dsDNA antibodies are reactive to cell surface annexin II and through this interaction, anti-dsDNA antibodies are bound and then internalized and translocated into the cytoplasm and/or nucleus where they mediate altered cellular functions. Compositions that inhibit or interfere with the interaction of annexin II with anti-dsDNA antibodies can be used to treat one or more symptoms or pathological processes of an inflammatory or immunological disorder, preferably an auto-immune disorder. Methods for monitoring the progression or severity of an inflammatory or immunological disorder are also provided. In certain embodiments, levels of annexin II and/or anti-dsDNA antibodies, including anti-dsDNA antibodies that can bind to annexin II, are assessed and compared to a reference level of annexin II and/or anti-dsDNA antibodies that corresponds to a specific stage or severity of the disorder.
CN101732555A Medicament for treating cold cough and chronic bronchitis The invention discloses a medicament for treating cold cough and chronic bronchitis, which adopts the technical scheme that the medicament comprises the following components in part by weight: 30 to 70 parts of unibract fritillary bulb, 30 to 70 parts of platycodon root, 200 to 500 parts of loquat leaf, 0.2 to 0.6 part of menthol and 0.5 to 5 parts of almond essence; and a method for preparing granular formulations of the medicament comprises the steps of: in the medicaments, pulverizing the unibract fritillary bulb into fine powder in an ultramicro mode; pulverizing the platycodon root into fine powder in an ultramicro mode and sieving the powder with a 200-mesh sieve; decocting platycodon root coarse powder and the loquat leaf by adding water, then uniformly mixing the mixture and the platycodon root fine powder, drying and porphyrizing, adding the unibract fritillary bulb fine powder into the mixture, and uniformly mixing to prepare granules; and drying the granules, adding the almond essence, the menthol and starch, uniformly mixing and encapsulating. The medicament has the advantages of treating cough yellow sputum or unsmooth expectoration, throat gall, chest distress and swelling pain, cold cough and chronic bronchitis which are caused by wind-heat affecting lung and fire transmission from internal depression. The extracted medicament is prepared into formulations such as capsules or soft capsules, micro-capsules or pills, is convenient for popular use, and reduces paraesthesia during administration.
US20080249043 Methods and Compositions Involving Protein Kinase C-Delta Disclosed are methods and compositions relating to the use of PKC-δ activators in the treatment of disease.
US8207160 Tetrahydrobenzazepines and their use in he modulation of the dopamine D3 receptor The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.
WO2008055317A1 Compositions and methods for the treatment of prostate cancer A pharmaceutical composition for inhibiting the proliferation of prostate cancer cells, said composition comprising a synergistic combination of a therapeutically effective amount of at least one COX inhibitor, and either one or both of: (a) at least one LOX inhibitor (b) at least one cPLA2-α inhibitor.
CN102028731A Medicine powder applied through nose and used for treating migraine The invention discloses medicine powder applied through a nose and used for treating migraine. The medicine power comprises the following components in parts by weight: 100 to 150 parts of dahurian angelica root, 50 to 80 parts of manchurian wildginger, 30 to 60 parts of borneol and 100 to 150 parts of Szechuan lovage rhizome. The medicine powder treats the migraine after being applied through the nose, and has the advantages of rapid effect, accurate treatment effect, simple method and low cost.
US20050042296 Superfine aqueous dispersion of noble metal for head massage When micro-dispersion water containing super-fine noble metal particles, as produced by causing plasma discharge in water between a noble metal electrode and its counter electrode, is applied to the scalp and the head is massaged, such solution will permeate through the hair roots into the hair tissues in the scalp all the way to the hair matrix cells and hair papilla, thereby transferring the beneficial effects of such solution to the tissue nerves and capillary vessels to activate the brains.
US20080275053 Heterocyclyl Compounds Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R1, R2a, R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
US20080058409 Esterified Catechins, Processes for Producing the Same, and Foods and Beverages as well as Cosmetics Containing Such Esterified Catechins The present invention provides substances having sufficiently antibacterial activity against heat-resistant spore-forming bacteria that they can be used to improve the shelf life of beverages and processed foods, as well as to control the growth of microorganisms in cosmetics. The present invention provides a catechin ester in which at least one of the hydroxyl groups of a catechin is esterified with a medium-chain fatty acid. This medium-chain fatty acid ester of a catechin, which may be used either alone or as a composition, shows a strong growth suppressing effect on heat-resistant spore-forming bacteria and, if added to foods or beverages, can prevent them from rotting or deterioration and, if added to cosmetics, can prevent their rotting or deterioration.
US20100113575 Method for detecting autoprocessed, secreted pcsk9 The present invention provides a method for detecting autoprocessed, secreted PCSK9, a protein involved in cholesterol homeostasis, and for effectively identifying compounds that inhibit autocleavage and secretion from cells. The disclosed method involves the insertion of an epitope tag into a PCSK9 expression construct immediately C-terminal to the pro domain ending at an amino acid residue corresponding to Q152 of human PCSK9. Upon autoprocessing, the epitope tag is exposed and capable of recognition by anti-epitope antibodies or other suitable identification system, allowing for the selective and exclusive identification and/or quantification of processed PCSK9. The present disclosure thus advances the goal of providing enabling technology to the art for the effective identification of therapeutics effective in combating coronary heart disease.
CN103665175A Fructan extract, and preparation method and application thereof The invention discloses a fructan extract and a preparation method thereof. The preparation method comprises the following steps: extracting Sichuan ophiopogon root tuber with ethanol to remove impurities, extracting with water, carrying out ethanol fractional precipitation, and drying to obtain a fructan extract (the molecular weight is 2500-8000). The method for preparing the fructan extract has the advantages of short time consumption and low cost, and can perform abundant preparation and adapt to industrial production. Besides, the invention also discloses application of the fructan extract in preparing medicines, foods or health products for losing weight. The inspection on functions of the fructan extract by a diet-induced fat mouse model proves that the fructan extract has an obvious action of losing weight.
CN102786538A Salicylaldehyde glycine Schiff base and o-phenanthroline copper (II) coordination compound and preparation process and application thereof The invention discloses a salicylaldehyde glycine Schiff base and o-phenanthroline copper (II) coordination compound which has a structure as follows. A preparation process of the coordination compound comprises the steps of dissolving 1-2mmol of glycine and 1-2mmol of potassium hydroxide in 5-10mL of absolute methanol, heating and stirring till the solution is dissolved fully; then dropwise adding 5-10mL of a methanol solution containing 1-2mmol of salicylaldehyde in the solution, stirring continuously, and conducting a reflux reaction for 1-2 hours at a temperature between 50 DEG C and 70 DEG C; and adding 2-4mL of 0.50mol/L copper acetate aqueous solution, conducting the reflux reaction for 2 hours, adding 0.2-0.4g of o-phenanthroline, conducting the reflux reaction for 3 hours, cooling, filtering to obtain grass green precipitates, so that the salicylaldehyde glycine Schiff base and o-phenanthroline copper (II) coordination compound is obtained. The salicylaldehyde glycine Schiff base and o-phenanthroline copper (II) coordination compound has the advantages of being high in anticancer activity, good in lipid solubility, low in cost, simple in preparation process and the like, can be used for preparing drugs for treating human liver cancer and human lung adenocarcinoma and provides a new path for development of anti-cancer drugs.
CN102516324A Glycosyl ester compound and preparation method and application thereof The invention discloses a glycosyl ester compound and a preparation method and application thereof. The glycosyl ester compound has a molecular formula of C16H26O8. The preparation method comprises steps of: placing a whole plant or tissues of Portulaca oleracea Linn. into organic solvent for digestion; separating to obtain a leaching liquor, extracting the leaching liquor and concentrating the extract to obtain extractives; and carrying out chromatography separation and purification on the extractives too prepare the glycosyl ester compound. The organic solvent is one or two selected from methanol, ethanol, n-butyl alcohol and acetone. The invention obtains a glycosyl ester compound with a novel structure from Portulaca oleracea Linn. through extraction and separation. The compound has good anti-tumor activity and can be applied to preparation of anti-tumor medicament or healthful food for preventing tumor and has good development prospect.
WO2013011858A1 Tetravalent platinum complex and pharmaceutical composition containing same [Problem] To provide a novel tetravalent platinum complex characterized by having a high anti-tumor activity on malignant tumors and has relatively reduced adverse side effects. [Solution] A tetravalent platinum dichloromalonic acid salt complex characterized by having cis, cis-spiro[4,4]nonane-1,6-diamine or an optical active diamine thereof, particularly (S,S,S)-cis, cis-spiro[4,4]nonane-1,6-diamine represented by formula (G), as a ligand.
WO2008033432A3 Immune modulation by chemically modified ribonucleosides and oligoribonucleotides The invention relates to modified oligoribonucleotides with immunomodulatory activity. The invention encompasses treatment of autoimmune and infectious diseases using the oligonucleotides of the invention.
WO2010127363A1 Toposiomerase inhibitors The invention provides compounds of formula I: (I) wherein A, B, W, Y, Z, R1 R3 and R4 have any of the meanings defined in the specification and their salts as well as additional compounds and their salts. The invention also provides pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for preparing compounds of the invention, and therapeutic methods for treating cancer, a bacterial infection or a fungal infection using compounds of the invention.
WO2009004990A1 Fp receptor agonist It is intended to provide a prostaglandin F2α receptor agonist (FP receptor agonist), which comprises a biphenyl derivative represented by the following general formula (I) (wherein m represents an integer of 0 to 2; n represents an integer of 0 to 5; R1 represents optionally substituted lower alkyl, optionally substituted lower alkanoyl, etc.; R2 represents optionally substituted lower alkyl, optionally substituted lower alkoxycarbonyl, an optionally substituted aliphatic heterocyclic group, etc.; and R3 represents a halogen, optionally substituted lower alkyl, optionally substituted lower alkoxy, etc.;)or a pharmaceutically acceptable salt thereof as the active ingredient, and so on: (I)
US20080038305 Ceramic Bulking Agent This invention relates to a tissue bulking agent comprising a particulate micro-porous bioinert ceramic material, in the form of spheres, having interconnected pores. Pores on the surface of each sphere are connected to pores inside such sphere via blow-holes and the internal pores are in turn interconnected, so that in addition to a high porosity, the spheres have a high permeability to gas and liquid. The bulking agent is disposed inside a syringe and is activated by impregnating the particles with traces of a bioactive resorbable bioceramic or by the in situ impregnation with serum from the blood of a patient. The particles are mobilised for injection by mixing the particles with a bio-suitable carrier gel or a viscous, lubricating carrier liquid. Thereafter, the activated and mobilised bulking agent is injected into the tissue in the area to be treated or bulked, such as the pelvic floor or urinary sphincter.
WO2014060742A1 Tert-butyl n-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2h)-yl]-3,5- difluorophenyl}ethyl]-l-alaninate or a salt, hydrate or solvate thereof The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5- (2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2- oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.
WO2009038812A1 Condensed piperidine derivatives useful as vanilloid receptor ligands Bicyclic 3,4-fused piperidiπe compounds having the structure of formula (I) and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, differentiation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
WO2007098091A3 Treatment of hyperproliferative diseases with vinca alkaloid n-oxide and analogs The present invention relates to vinca alkaloid and analog N-oxides having activity for treating hyperproliferative disorders. Further, the invention relates to pharmaceutical compositions and methods of using vinca alkaloid and analog N-oxides, alone or in combination with one or more other active agents or treatments, to treat hyperproliferative disorders.
CN1824050B Applicaiton of a composition for preparing medicine and food dual purpose nutritive product for preventing and treating xeroma A medical product used as both medicine and food for preventing and treating the xerophthalmia caused by pantatrophia is prepared from composite medicine, vitamins and trace elements. Its preparing process is also disclosed.
US7109166 A piperazine-somatostatin analog in sustained release ionic conjugate with lactic acid-glycolic acid-tartaric acid copolymer; for therapy of gastrointestinal disorders, such as Crohn's disease, systemic sclerosis, external and internal pancreatic pseudocysts and ascites, VIPoma, nesidoblastosis This invention is directed to a sustained release composition comprised of Compound (A) having the formula or a pharmaceutically acceptable salt thereof, and a copolymer comprised of poly-(I)-lactic-glycolic-tartaric acid wherein the amino group of Compound (A) is ionically bound to a carboxyl group of the copolymer and wherein further the composition may be made into a sustained release pharmaceutical composition with pharmaceutically acceptable carrier(s).
CN102232944A Antrodia cinnamomea pimelie kelone compound for inhibiting growth of oral cancer tumor cells The invention relates to a new use of a compound, and a medical composition for inhibiting growth of oral cancer tumor cells. A antrodia cinnamomea extract is subjected to separating and purifying to prepare 4-hydroxy-2,3-dimethoxy-6-methy-5(3,7,11-trimethyl-dodeca-2,6,10-trienyl)-cyclohex-2-enone. The pimelie kelone compound can be provided for inhibiting the growth of the oral cancer tumor cells. Meanwhile, the pimelie kelone compound can be provided for preparing the medical composition for inhibiting the growth of the oral cancer tumor cells.
US7902358 Gastrointestinal disorders; inflammatory bowel disorders; gastroesophageal reflux, constipation; diarrhea The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
US7405206 Administering by inhalation; antiinflammatory agents, antiallergens; skin disorders; reacting androstane compound with 2-oxofuran compound There are provided compounds of formula (I) wherein R1 represents O, S or NH; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the α or β configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond; and salts and solvates thereof; process for preparing them, compositions containing them and their use in therapy.
CN1965823B (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4 acetylaminoisoindoline 1,3-dione, its preparation method and its compound Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (-) isomer, and prodrugs, metabolites, polymorphs, salts,solvates, hydrates, and clathrates thereof are discused. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF- alpha or the inhibition of PDE4.
WO2007069924A1 Deazapurine analogs of 4'-aza-l-nucleosides The invention relates to compounds of the formula (I), which are L-enantiomeric forms of nucleoside analogues, and to pharmaceutical compositions containing the compounds, methods of treating certain diseases, including cancer, bacterial infection, parasitic infection, and T-cell mediated diseases, using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds.
CN101744882A Medicament for treating penile erectile dysfunction The invention discloses a medicinal composition for treating penile erectile dysfunction. The invention is characterized in that the medicinal composition comprises the following raw material medicaments: danshen root, sanchi and borneol. The pharmacological test and the clinical experiment show that the medicament of the invention has the advantages of little side effect, wide therapeutic window and the like; the administration of the medicament cannot generate after effect on the patient; the medicament has characteristics of natual medicaments; and the medicament of the invention has good pharmacological effects.
CN103040790A Preparation method of wild cactus polysaccharide poly(lactic-co-glycolic acid) (PLGA) microcapsules The invention relates to wild cactus polysaccharide poly(lactic-co-glycolic acid) (PLGA) microcapsules and a preparation method thereof. PLGA is taken as a coating material for the wild cactus polysaccharide microcapsules. The preparation method comprises the following steps of: (1) dissolving wild cactus polysaccharide into water to form an inner aqueous phase; (2) dissolving the PLGA into an organic solvent to form an oil phase; (3) adding the inner aqueous phase into the oil phase for pre-emulsification, thus obtaining pre-emulsion; (4) adding the pre-emulsion into an outer aqueous phase for re-emulsification, thus obtaining re-emulsion; (5) adding the re-emulsion into a NaCl solution, volatilizing the organic solvent by stirring, and curing microcapsules; and (6) centrifuging, collecting, washing and freeze-drying the microcapsules after the stirring is stopped, thus obtaining the wild cactus polysaccharide PLGA microcapsules. The prepared wild cactus polysaccharide PLGA microcapsules are uniform in size, smooth in surface and high in entrapment efficiency.
WO2009085651A1 Metal carbonate particles for use in medicine and methods of making thereof Silver-containing particles, and methods of making silver-containing particles are disclosed.
US20130079401 Novel use of isothiocyanates for treating cancer Novel Uses of small molecules, particularly, 6-methylsulfinylhexyl isothiocyanate and 6-methylsulfonylhexyl isothiocyanate, are disclosed herein. The two isothiocyanates are useful as lead compounds for manufacturing a medicament or a pharmaceutical composition for treating cancer, particularly drug-resistant cancer, in a patient.
CN101474281B Pain-eliminating paste for zoster and preparation method thereof The invention discloses a pain-relieving ointment for shingles and a preparation method thereof. The parts by weight of the components are as follows: 20-40 parts of phellodendron, 20-40 parts of coptis root, 20-40 parts of rheum officinale, 3-8 parts of centipede, 20-40 parts of natural indigo, 20-40 parts of red orpiment, 20-40 parts of borneol, 15-35 parts of prepared frankincense, 15-35 partsof prepared myrrh, 800-1,200 parts of sesame oil, and 50-80 parts of white wax. The centipede, natural indigo, red orpiment, borneol, prepared frankincense and prepared myrrh are ground into fine powder, mixed and added into the extract of phellodendron, coptis root, rheum officinale and sesame oil, then the ointment is prepared. The invention has the advantages of full play of drug effects, longduration, excellent pain-relieving effect and reduced occurrence rate of postherpetic neuralgia.
CN102351705A Propylgallate compound and pharmaceutical composition thereof The invention relates to a propylgallate compound. Through powder X-ray diffraction measurement, the characteristic diffraction peaks of the propylgallate compound are shown in 8.2 degrees, 9.8 degrees, 13.3 degrees, 14.8 degrees, 16.9 degrees, 21.3 degrees, 22.0 degrees, 23.3 degrees, 24.6 degrees, 25.9 degrees, 30.1 degrees, 32.0 degrees, 33.0 degrees and 34.7 degrees in the X-ray powder diffraction pattern represented by the diffraction angle of 2theta+/-0.2 degree; and the propylgallate compound has the melting point of 140-142 DEG C. The invention also relates to a preparation method of the propylgallate compound, and a pharmaceutical composition containing the propylgallate compound. The pharmaceutical composition comprises the propylgallate compound and pharmaceutically acceptable carriers.
CN101502517A Glipizide enteric sustained-release preparation composition and method for preparing the same The invention discloses a glipizide enteric sustained-release preparation combination and a preparation method thereof. The glipizide enteric sustained-release preparation combination is mainly prepared from glipizide bulk drugs, sustained-release materials, enteric materials and other appropriate auxiliary materials. The glipizide enteric sustained-release preparation provided by the invention can not only prevent glipizide from disintegrating in the stomach and causing irritation to gastric mucosa and avoid the adverse reactions caused by the administration, such as nausea, abdominal pain, diarrhea and the like, but also deaccelerate the release rate of drugs, reduce the frequency of administration and improve the patient compliance. The invention provides a novel form of drug featuring higher safety and better patient compliance and having the advantages of high quality controllability and stability of the preparation process.
US20110091538 Polymer adapted to release bioactive agents in vivo, pharmaceutical composition and method of preparation thereof The present invention provides a Monodisperse Polymer Particles (MPP) adapted to release alkoxy groups by means of a hydrolyser, such that Monodisperse Bioactive Polymer Particles (MBPP) are obtained in vivo. The MBPP are characterized by (a) at least one naturally occurring or synthetic long molecular chain consisting of biologically stable backbones optionally crosslinked, further characterized by a molecular weight of at least 1 KD, comprising between 10 to 1,000,000 repeated covalently-linked small molecules with a functionality of at least one alkoxy releasing group per molecule; (b) a long dimension between 0.1 and 10 micrometers; and, (c) a zeta potential value of 30 to 130 mV at pH of about 7.0. The MBPP alter, inhibit, activate, induce or otherwise affect biological or chemical events in vivo.
CN101530561A Hemostyptic medicine The invention relates to a hemostyptic medicine, which can effectively solve the problems of slow hemostyptic speed, easy infection, toxic and side effects, high price, complicated hemostyptic process and small application range. The solving technical proposal of the invention is that: the hemostyptic medicine is prepared by the following raw material drugs by weight: 9 to 11g of colophony, 18 to 22g of white vitriol, 4.5 to 5.5g of sanguisorba, and 4.5 to 5.5g of bletilla, wherein the colophony and half white vitriol are respectively crushed into colophony powder and white vitriol powder for standby; the sanguisorba and the bletilla are burnt into char respectively and are crushed into sanguisorba powder and bletilla powder for standby; the rest half white vitriol are of bulge shape after heating, namely calcined alum; the calcined alum are crushed, and are evenly mixed with the colophony powder, the white vitriol powder, the sanguisorba carbon powder and the white bletilla powder to prepare the hemostyptic medicine. The hemostyptic medicine has the advantages of convenient use, low cost, fast hemostyptic speed, infection prevention, and is an innovation in the medicament field.
US20110136794 Novel pyrrole derivative having, as substituents, ureido group, aminocarbonly group and bicyclic group which may have substituent A compound represented by the following formula (1) or a salt thereof: The compound has an inhibitory activity on the production of interleukin-6, and is therefore useful as a preventive and/or therapeutic agent for a disease associated with interleukin-6, ocular inflammatory diseases and the like. In the formula, R1 represents a halogen atom, a hydrogen atom, a lower alkyl group which may have a substituent, a formyl group, or a lower alkylcarbonyl group which may have a substituent, R2 represents a bicyclic hydrocarbon group which may have a substituent or a bicyclic heterocyclic group which may have a substituent, R3 represents a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, or an acyl group.
WO2009040816A1 Methods of treating lysosomal storage disorders The sphingolipid storage disease (SLSD) is selected from the group consisting of Gaucher' s Disease, Niemann-Pick Disease, Krabbe' s Disease (Globoid leukodystrophy), Metachromatic leukodystrophy, Ceramide lactoside lipidosis, Fabrys Disease, Tay-Sachs Disease, Sandhoffs Disease and Landing's Disease. The cholesterol synthesis inhibitor is selected from the group consisting of mevastatin, lovastatin, pravastatin, fluvastatin, simvastatin, rosuvastatin, cerivastatin and atorvastatin.
US20060058346 Novel enantiomers of etrahydroisoquinoline derivatives and theirpharmaceutically acceptable salts, their preparations and pharmaceutical compositions The disclosure concerns novel enantiomers of tetrahydroisoquinoline derivatives and their pharmaceutically acceptable salts, their preparations and pharmaceutical compositions. The enantiomers of tetrahydroisoquinoline derivatives are provided which are useful in stimulating heart rate and hypotensive activity, inhibitory activity against platelet aggregation, and suppressive against inducible NO synthase. The enantiomers of tetrahydroisoquinoline derivatives and their pharmaceutically acceptable salts are effective for treating congestive heart failure, hypertension, thrombosis, inflammation, septicemia, cardiac insufficiency, and disseminated intravascular coagulopathy.
CA2602776C Method for treating prostate diseases based on local delivery of active substances A method for treating prostate related diseases in a subject, the method comprising i) optionally administering to subject an initial boost dose of one or more active substances and/or prodrugs, and ii) administering locally into the prostate a controlled release pharmaceutical composition comprising one or more active substances in a biodegradable ceramic carrier. The biodegradable hydrating ceramic may be selected from the group consisting of non-hydrated or hydrated calcium sulphate, calcium phosphate, calcium carbonate, calcium fluoride, calcium silicate, magnesium sulphate, magnesium phosphate, magnesium carbonate, magnesium fluoride, magnesium silicate, barium sulphate, barium phosphate, barium carbonate, barium fluoride, barium silicate, or mixtures thereof. In a specific embodiment, the biodegradable hydrating ceramic is non-hydrated or hydrated calcium sulphate.
US20080227764 E.g., 3,-30-pregnanediones or 11,20-pregnanedioles; optionally in association with one or more other analgesic compounds such as opioids; does not result in overt sedation The present invention relates to the use of pregnanes in inducing analgesia, preferably without overt sedation, in a mammal in response to neuropathic pain, and compositions and kits therefore.
WO2013050527A1 Quinazoline derivatives as pde10a enzyme inhibitors This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
US20070275002 Use Of Proteins And Peptides Encoded By The Genome Of A Novel Sars-Associated Coronavirus Strain The invention relates to the use of proteins and peptides coded by the genome of the isolated or purified strain of severe acute respiratory syndrome (SARS)-associated coronavirus, resulting from sample reference number 031589 and, in particular, to the use of protein S and the derivative antibodies thereof as diagnostic reagents and as a vaccine.
CN102895201A Valproate semisodium tablet and its preparation method The invention provides a valproate semisodium tablet and its preparation method. The common valproate semisodium tablet comprises 50-67wt% of valproate semisodium, 25-35wt% of a microcrystalline cellulose, 5-9wt% of lactose, 1-3wt% of sodium carboxymethyl starch, 0.2-2wt% of magnesium stearate, and 1-10wt% of silica and/or talcum powder. The valproate semisodium tablet has the advantages of stable quality, no fractured, cracked or crushed tablets, and realization of the enteric-coated tablet release degree according with requirements of Chinese Pharmacopoeia 2005. The preparation method obviously overcomes the disadvantages comprising bad particle fluidity, sticking, tablet breaking and tablet appearance disqualification in present production technologies, has no special requirements on the production environment, enables the qualification rate of products to reach above 95%, and is suitable for large-scale industrialized production.
CN1951907A Compound and its preparation method and its application in pharmacy The invention discloses a compound and preparing method and application in the drug, which is 2, 3-diamino-6-hydroxy-benzene carbonic acid-2-ethyl group-hexaester fermented by M 206095 strain with excellent antimycotic action to prepare antimycotic drug.
CN102391283A Clopidogrel hydrogen sulfate compound and preparation method thereof The invention relates to a clopidogrel hydrogen sulfate compound preparation method which comprises the following processing steps of: 1) dissolving raw clopidogrel hydrogen sulfate in water, adjusting pH by using sulfuric acid, adding organic solvent for extraction and then separating an organic phase to obtain a primary purified aqueous phase containing the clopidogrel hydrogen sulfate; 2) adding activated carbon into the aqueous solution, filtering to collect filtrate, cooling the filtrate, filtering and concentrating the filtrate dry; and 3) separating and purifying the samples through a preparation-type neutral alumina chromatographic column, collecting eluent, concentrating and spray drying to obtain tertiary purified clopidogrel hydrogen sulfate. The preparation method has the advantages that the quality of products is improved, the toxic and side effects during the preparation of platelet aggregation inhibitor drugs are reduced and the method is suitable for large-scale industrialized production.
US20080221103 4-(3-Methyl-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-ylamino)-6-(methylthio)-2-phenylpyrimidine-5-carbonitrile; having significant in vitro TNF- alpha inhibitory activity useful for the treatment of various inflammatory diseases such as arthritis, inflammatory bowel disease, psoriasis, asthma, COPD, cancer etc. Provided herein are heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as described herein. Further described herein in particular are heterocyclic compounds of the formula (I) for treating various diseases. and disorders by administering in a patient one or more TNF-α, Thromboxane synthase, 5-LOX, and PDE4 inhibitors. In particular described herein are methods for treating immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; ischemic heart disease; atherosclerosis; cancer; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; cachexia; asthma; bone resorption diseases; ischemia reperfusion injury; brain trauma; multiple sclerosis; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection and diseases mediated by HIV-1; HIV-2; HIV-3; cytomegalovirus (CMV); influenza; adenovirus; the herpes viruses (including HSV-1, HSV-2) and herpes zoster viruses in a mammal comprising administering an effective amount of a compound of formula (I).
EP1763530A1 Imidazopyridazine diones, the production thereof, and the use of the same as a medicament The invention relates to substituted imidazopyridazine diones of general formula (I) wherein R1 to R4 have the designation defined in patent claim 1. The invention also relates to the tautomers, enantiomers, diastereomers, mixtures and salts of said diones, comprising valuable pharmacological properties, especially an inhibitive effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
US20080153167 In vivo amplification of neural progenitor cells The invention is directed to methods for in vivo amplification of neural progenitor cells using the proliferative environment of glial neoplasms in adult brain. The progenitor cells have the capacity to proliferate and differentiate into mature brain cells which can be used for cell replacement therapies. The invention also provides cell replacement therapy methods for treating central nervous system diseases or injuries, including multiple sclerosis, stroke, Alzheimer's disease and Parkinson's disease.
CN101366920A Prick removing lozenge for laryngopharynx and preparation The invention provides a buccal tablet for removing spur in throat and a method for preparing the same. The buccal tablet is characterized in that the buccal tablet is a carbohydrate buccal tablet which can soften bony spur, diminish inflammation, alleviate pain, stanch blood and dissipate blood stasis, and is formed by a nanometer material for dissolving bony spur in the throat; the preparation method comprises the following steps: firstly, hawkthorn dry powder, ebony dry powder, lemon dry powder, borneol, bletilla striata, dextrin and cyclamate are respectively dried, pulverized, put together and evenly stirred; the fineness is controlled below 100 meshes; secondly, the mixture is put into an airflow pulverizer and machined to a powder body with the fineness of between 500 and 2,000 nanometers; and finally, the powder body is prepared to a sugar-coated spherical particle or flaky particle tablet, and each particle is 5 grams, that is the product of the invention.
CN101732358A Method for proliferating bifidobacteriums in human and animals bodies The invention discloses a method for proliferating bifidobacteriums in human and animal bodies and belongs to the field of human and animal microecology, and more specifically belongs to the field of human and animal enteric canal microecology. The method adopts aerobes which are beneficial to human or animals to consume oxygen in the digestive systems, especially in the enteric canals of human and animals and to create an oxygen-free environment for the growth and proliferation of the bifidobacteriums in the enteric canals, thus enhancing the proliferative effect of bifidus factors towards the bifidobacteriums in the enteric canals or reducing the intake of the bifidus factors. The intake of aerobes which are beneficial to human or animals can be carried out before the intake of the bifidus factors, or the two can be taken in simultaneously. The main purpose of the method is to increase the quantity of bifidobacteriums in human and animal bodies and to improve human and animal health.
CN101524406A New formula for removing aldehyde in solution The invention discloses a formula for removing aldehyde in solution. The formula contains the following materials by weight parts: 80 to 120 of vitamin C, 15 to 25 of nicotinic acid, 2 to 4 of vitamin B, 80 to 120 of butanedioic acid, 80 to 120 of fumaric acid, 400 to 600 of L-cysteine, 160 to 240 of L-lactamine, 160 to 240 of L-glutamic acid, 80 to 120 of lipoic acid, 180 to 240 of pyruvic acid and 8 to 12 of cassia stem. The formula can be used for preparing tablets, medicinal granules, capsules, oral liquid or beverages. The invention has reasonable formula, the formula composition fully utilizes own characteristics of all the components; reasonable combination leads the formula to exert a comprehensive curative effect; and by experimental verification, the formula has the effect of removing aldehyde in solution fast.
WO2008030511A2 Substituted 3,4,6,7-tetrahydro-5h, 1,2a,4a,8-tetraazacyclopenta[cd]phenalenes Substituted 3,4,6,7-tetrahydro-5H-1,2a,4a,8-tetraazacyclopenta[cd]phenalene-9-amines of formula (I), pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
CN101381371A Dithiolopyrrolones compounds and preparation method and application thereof The invention discloses a dithiole-pyrrollidone compound shown in a formula I and a pharmaceutically acceptable salt thereof, wherein X is O, NR4 or S; R1 can be any of the following unsubstituted or substituted groups a cycloalkyl group having 3 to 8 carbon atoms, an aromatic group having 5 to 10 carbon atoms or a heterocyclic group having 3 to 10 carbon atoms as well as 1 to 3 atoms selected from a nitrogen atom, an oxygen atom or a sulfur atom; R2 can be either of hydrogen and an alkyl group having 1 to 10 carbon atoms; R3 can be hydrogen or any of the following unsubstituted or substituted groups: an alkyl group having 1 to 10 carbon atoms, an alkenyl having 2 to 10 carbon atoms, an alkynyl group having 2 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms, an alkyl group having 1 to 10 carbon atoms as well as an aromatic group with 5 to 10 carbon atoms, an aromatic group having 5 to 10 carbon atoms or heterocyclic group having 3 to 10 carbon atoms as well as 1 to 3 atoms; and R4 can be either of hydrogen or an alkyl group having 1 to 10 carbon atoms. The invention also discloses a preparation method and application to preparation of drugs for increasing peripheral blood white cells and preparation of ancillary drugs for phrohibiting the reduction in peripheral blood white cells during radiation treatment or chemo-treatment. The compound of the invention has the function of quickly and continuously increasing the peripheral blood white cells.
CN101422534A Radio therapy sensitization composite preparation The invention discloses a radiotherapy and enhancement combination preparation which is an oral liquid preparation prepared by cordycepin, wolfberry olysaccha prides, lingzhi spore and aloe extract. The combination preparation has no toxic side effect; all the components are processed and then combined, and promote each other in function. The combination preparation can be taken for strengthening the body resistance to consolidate the constitution of patients, fully protect normal cell from being damaged, actively adjust immunologic function, assist to kill tumor cells and enhance the radiotherapy effect.
WO2007043365A1 Therapeutic agent for neurogenic pain Disclosed is a therapeutic agent for neurogenic pain, which has an excellent therapeutic effect on neurogenic pain which is an intractable disease. Specifically, disclosed is a therapeutic agent for neurogenic pain or a pharmaceutical composition for the treatment of neurogenic pain which comprises, as an active ingredient, (1) a compound having an anti-progesterone activity (e.g., fulvestrant (ICI182.780), fluocinolone acetonide, triamcinolone acetonide), (2) a compound having an estrogenic activity (e.g., 17β-estradiol) or (3) a mixture of a compound having an anti-progesterone activity and a compound having an estrogenic activity (e.g., 17β-estradiol and fulvestrant). Also disclosed is a method for treatment of neurogenic pain by using any one of the compounds.
CN103709150A A besigliptin tosilate crystal form, a preparation method there and applications thereof The invention discloses a besigliptin tosilate crystal form, a preparation method there and applications thereof. XRD spectrum characteristic peaks 2(+/-0.2 degree) of the besigliptin tosilate crystal form are 6.07, 8.78, 12.04, 13.62, 13.62, 18.75, 19.13, 20.02 and 24.96. The crystal form provided by the invention is good in stability.
CN101161234A Erlotinib sustained-release implants for treating entity knub An erlotinib slow release implant for treating solid tumor is characterized in that the slow release implant contains anti-cancer effective amount erlotinib, slow release supplementary materials and some slow release regulator. The solid tumors comprise esophagus cancer, stomach cancer, breast cancer, ovarian cancer, prostatic cancer, bladder cancer, liver cancer, lung cancer and colorectal cancer. The slow release supplementary materials mainly are one or their combination of co-polymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate), and poly (L-lactide-co-propyl phosphate), during its degradation and absorption, slow releasing erlotinib to tumor local, so it greatly decreases its whole body toxicity reaction, at the same time it also maintains effective medicine concentration of tumor local. The tumor local is arranged with the slow release implant, which can not only decrease whole body toxicity reaction of erlotinib, but also selectively promote medicine concentration of the tumor local, reinforce therapeutic effect of non-operation therapy such as chemotherapeutic drugs, radiotherapy and etc.
CN103417741A Medicated wine for rectifying qi and dispersing phlegm The invention discloses medicated wine for rectifying qi and dispersing phlegm. The medicated wine is characterized by comprising the following ingredients: 5 g of kelp, 55 g of seaweed, 5 g of agilawood, 6 g of realgar, 1 g of endoconcha sepiae, 10 g of asarum sieboldii, 10 g of aristolochiae lignum, and 800 ml of Chinese spirits. The medicated wine allows the formula ingredients to play a synergistic effect, can be targeted on rectifying qi, dispersing phlegm and removing stasis, also has simple manufacture, significant effect and low cost, and is beneficial to the health of people.
EP2345636A1 Casr agonist By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.
US20070021483 Amidine derivatives for treating amyloidosis The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an amyloid-related disease in a subject comprising administering to the subject a therapeutic amount of an amidine compound. Among the compounds for use according to the invention are those according to the following Formula, such that, when administered, amyloid fibril formation, neurodegeneration, or cellular toxicity is reduced or inhibited:
US20050124640 Pyrimidine derivatives useful as inhibitors of PKC-theta Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
US7220561 Using transgenic bacillus to ferment vitamin b5, valine and isoleucine The present invention features improved methods for producing pantoate and pantothenate utilizing microorganisms having modified pantothenate biosynthetic enzyme activities. In particular, the invention features methods for reducing byproduct formation and increasing yields and purity of desired product. Recombinant microorganisms and conditions for culturing same are also are featured. Also featured are compositions produced by such microorganisms.
CA2504207C New amide compounds having mch-antagonistic activity and medicaments comprising these compounds The present invention relates to amide compounds of general formula I (See Formula I) wherein A, B and Y are carbo- or heterocyclic groups; b is 0 or 1; X is an alkylene bridge; W is alkylene, alkenylene, alkyloxy, alkylamino, etc.; Z is a bond or alkyiene bridge; R1, R2 and R3 are hydrogen, alkyl, cycloalkyl, etc., or R1 and R2 form an alkylene bridge. Moreover the invention relates to pharmaceutical compositions containing at least one amide according to the invention. In view of the MCH receptor-antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
US20080255132 Combination Therapy Comprising the Use of Et-743 and Paclitaxel for Treating Cancer Methods of treating a human body for cancer are provided. In one aspect, an effective therapeutic amount of paclitaxel is administered in combination with ET-743 in a dose range between 0.5 and 1 mg/m2. In a related aspect, an effective therapeutic amount of ET-743 is administered in combination with paclitaxel in a dose range between 80 and 140 mg/m2.
WO2010006496A1 Compounds of estrogen-related receptor modulators and the uses thereof The compounds according to formula (I), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description.
CN101910155A Biphenyl derivatives as modulators of the histamine-H3 receptor useful for the treatment of disorders related thereto Biphenyl derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the H3 histamine receptor. (Ia) Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness, such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.
US20050182030 Antitumor, anticancer agents; osteoporosis; bone disorders; Paget's disorders; solution is provided in a sealed non-reactive plastic container of polypropylene, ABS, polyethylene, PVC, polycycloolefin; injectable, sterile, ready to use, pyrogen-free solution The present invention relates to an improved injectable ready-to-use preparation of pamidronate salts, methods for its manufacture and uses of the solution of the invention in the manufacture of pharmaceutical compositions for the treatment of diseases selected from the group of tumour-induced hypercalcaemia, Paget's disease, osteoporosis, bone metastases, or breast cancer. The ready-to-use solution comprises a physiologically acceptable alkaline salt of pamidronate which is water soluble and a physiologically acceptable aqueous solvent having a concentration of between 0.1 and 100 mg/mL, wherein the solution is provided in a sealed non-reactive plastic container.
US20100168210 T-Cell Cytokine-Inducing Surface Molecules and Methods of Use The invention provides cytokine modulators and methods for using the same to modulate cytokine production in monocyte lineage-derived cells. In particular, cytokine modulators of the invention selectively bind to a T-cell cytokine-inducing surface molecule (TCISM)-ligand of T lymphocytes or the corresponding TCISM-receptor of monocyte lineage-derived cells, thereby modulating cytokine production in monocyte lineage-derived cells.
WO2006014864A2 Methods and compositions for reducing c-reactive protein The present invention provides methods for the treatment and/or amelioration of inflammation in a subject, including humans, by administering to a subject a therapeutically effective amount of a biologically active mixture of high purity, high molecular weight straight chain primary aliphatic alcohols (referred to collectively herein as policosanol). Also included are methods of reducing levels of C-reactive protein in a subject, comprising administering to a subject a therapeutically effective amount of policosanol.
CN1923267A External-use gynaecologic antibacterial drugs and its preparing method The invention relates to a medicinal composition for treating gynaecologic diseases, which is prepared from raw materials including flavescent sophora root, roor of sessile stemona, gallnut, white alum, corktree bark and asarum through extracting and concentrating.
CN101536994A Method for preparing hybrid nanofiber membrane capable of loading drug The invention relates to a method for preparing a hybrid nanofiber membrane capable of loading drug. The technical scheme is as follows: the uniformly mixed hybrid nanofiber membrane is prepared at one step by using a two-channel or multi-channel axial flow injection pump and adopting the technology of high-pressure electrostatic spinning. The preparation method of the invention is simple, the surface of the obtained fiber membrane is smooth, fibers are uniform, and the diameters of the fibers range from 800 to 1200 nanometers.
CN102272126B Optical pure quinazoline compounds Optical pure quinazoline compounds, especially compounds of the general formula (I), wherein R1 and Y are defined as the specification, preparation methods of them, pharmaceutical compositions containing them and their uses are provided. Compounds of the general formula (VII), which are intermediates in the synthesis of the compounds of the general formula (I), wherein Ar, R2, R3, m, n, T and carbon atom with * are defined as the specification, are also provided.
WO2014095929A1 Composition and kit comprising piperazine derivatives and metformin, and use thereof in the treatment of diabetes The present invention relates to a composition comprising, in combination, metformin or a salt thereof, a pharmaceutically acceptable carrier or excipient and at least one compound of formula (I), the enantiomers, diastereoisomers or pharmaceutically acceptable salts thereof. Formula (I). The present invention also relates to the use of said composition for the treatment of diseases associated with insulin resistance syndrome.
CN101829144A Application of silica ultra-micropowder and drug for treating trachelitis The invention relates to application of a silica ultra-micropowder and a drug for treating trachelitis, belonging to the technical field of drugs. The invention discloses a drug for treating trachelitis and comprising a silica ultra-micropowder with effective dose and application of the silica ultra-micropowder in preparing a drug for treating trachelitis. The invention has the advantages that: a novel medical application is developed for the traditional silica ultra-micropowder, a novel application field is developed; the silica ultra-micropowder is safe and nontoxic, and has strong medicinal principle and better medicinal prospect; the raw materials of the product have abundant sources and low cost; the preparation process is simple; and the drug prepared by the product of the invention has a remarkable effect of treating trachelitis, has the cure rate of 100 percent, short treatment period and good safety because of being prepared by natural raw materials, wherein the trachelitis can be cured within 3 days.
CN102204867A Preparation method of liposome with functions of fat reduction and calcium supplement The invention discloses a preparation method of a liposome with functions of fat reduction and calcium supplement. The preparation method is characterized in that: on the basis of defining the therapeutic and health-care mechanism of a folk recipe, namely vinegar egg liquid, an ethanol injection method, an original sleeve dual-ejection technology and a homogenizing device with smeared sealing function are combined to reinforce the formation of the liposome of lecithin and the package of calcium acetate; the calcium acetate packaged by the liposome is transformed into ionic calcium hydroxide by transferring the liposome with the acetic acid through a calcium acetate gradient method; the liposome rich in the ionic calcium hydroxide is processed into an oral solution or freeze-dried powder. Compared with the traditional folk recipe, namely the vinegar egg liquid, the biological product developed by the method contributes more to massive production and long-term preservation and is more easy to absorb by a human body; the utilization of the calcium ions by the human body is greatly improved; the acidity of the human body is reduced; a healthy alkalescent environment is created in the human body; the fat-reducing function of the human body is enhanced; the target characteristic of softening blood vessels is more outstanding; and the therapeutic and health-care effect is more obvious.
CN102000033B Amoxicillin particle and preparation process thereof The invention discloses an amoxicillin particle and a preparation process thereof. In the preparation process of the amoxicillin particle, a low-moisture volatile adhesive solution and a cold drying technology are adopted. The invention has the advantages that the stability of the amoxicillin particle is enhanced; and within the 36-month valid period of the amoxicillin particle, the safety and validness of the amoxicillin particle in clinical use are ensured, and no penicillin anaphylaxis is generated.
WO2006116158A1 Benzodioxane and benzodioxolane derivatives and uses thereof Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R1, R2, R3, R4, y, n, m, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
CN103435612A Compound for treating diabetes mellitus The invention provides a compound shown in the formula I or pharmaceutically acceptable salts, hydrates or solvates thereof, and also provides new application of the compound or the pharmaceutically acceptable salts, hydrates or solvents thereof. A deuterated compound can be used for remarkably improving the conditions of the weight, fasting blood-glucose, transaminase and fasting serum insulin of an obese patient, increasing the insulin sensitivity can be improve, and enhancing the serum lipid parameter and oral glucose tolerance; the compound has the advantages that internal absorption effect is excellent;, the bioavailability is high, which is favorable for the taking of drug effect; the half-life period is prolonged, so that the administration frequency can be reduced and toxic and side effects can be reduced; therefore a new safe and reliable choice is provided to clinical administration. The formula I can be found in the specification.
CN1939333A Preparation of injecting soluble vitamines A process for preparing the injection of water-soluble vitamin includes such steps as thermally dissolving glycine in the water for injection while filling inertial gas, adding 12 compounds including cysteine hydrochloride, endrate disodium, vitamin C sodium, folic acid, etc, stirring, regulating pH=5.6-6.1, adding the water for injection, stirring, aseptic filtering, pouring in containers, pre-freezing, vacuumizing, filling inertial gas, pre-freezing, heating to 30-35 deg.C, holding the temp for 6-10 hr, filling inertial gas, and sealing.
WO2010015372A1 Pregnancy prevention using gestagens The invention relates to the use of at least one gestagen for producing an estrogen-free pharmaceutical for pregnancy prevention, wherein the pharmaceutical is intended for the daily administration of a pregnancy preventing dose of the at least one gestagen over a period of n x 21 days, where n = 1, 2, or 3, followed by an administration pause of 3 to 7 days, and to an associated method for pregnancy prevention and to an associated kit.
US20100249120 Substituted pyrazolo-pyrrolo-pyridine-dione compounds The present invention relates to substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
US7906483 Method for treating transplant rejection Compositions and methods for treating transplant rejection in a mammalian transplant recipient are provided. The method involves administering a therapeutically effective amount of Serp-1, its analogs, and biologically active fragments thereof in combination with an anti-rejection agent, such as cyclosporin, and a pharmaceutically acceptable carrier to a subject in need of such treatment. The compositions and methods are useful for treating acute and chronic allograft and xenograft transplant rejection in mammals.
CA2196690C Pregnanes and cholanes as neurochemical initiators of change in hypothalamic function The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a pregnane or cholane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.
WO2008051793A2 Method of preventing or treating metabolic syndrome Water-insoluble cellulose derivatives such as ethyl cellulose can be used to treat or prevent metabolic syndrome and/or one of the abnormalities of metabolic syndrome.
EP2687215A1 Mesterolone pharmaceutical composition for androgens' deficiencies in woman Mesterolone covers all indications for androgens in woman. Today Mesterolone is not prescribed for woman and its prescription is even exclusive for male patients. Mesterolone administration is prohibited for woman by the manufacturers because of risks of virilisation as opposed to what the invention shows when prescribed in physiological amount. Androgen's deficiencies in woman lead to ageing diseases to different degree: functional symptoms : hot flashes, irritability, intestinal distension, swollen legs. local consequences : sclerosis of bladder neck (chronic cystitis, incontinence, urgencies) sclerosis of vulva (painful or difficult copulation). general consequences : lipids' disorders; vascular disorders; weakness;hyper coagulation; venous thromboses; rheumatic problems; nervous breakdown; cerebral involution and Alzheimer's disease Depending from its molecular structure Mesterolone has properties similar to those of testosterone (influences general structures of the organism) Depending from its molecular structure Mesterolone has properties similar to those of dihydrotestosterone (influences local genital structures) Mesterolone is indicated for androgens' deficiencies in woman
US20110182886 Compositions and methods for inhibiting tumor progression Compositions and methods are provided for the classification, diagnosis, treatment, and prevention of tumors characterized by loss of REST function, expression of β2, and/or activation of Notch. Further compositions and methods are provided for modulation of cellular processes such as EMT, cell migration, and apoptosis.
CN102652757A Application of health-care drinking liquid containing deep seawater in preparation of medicaments or health-care products for preventing or treating metabolic syndrome The invention provides application of health-care drinking liquid containing deep seawater in preparation of medicaments or health-care products for preventing or treating metabolic syndrome. The health-care drinking liquid comprises liquid A and liquid B, wherein the liquid A is fresh water; and the liquid B is high-concentration concentrate obtained by reduced pressure concentration of concentrated water separated from the deep seawater through a reverse osmosis device, and the hardness range of the liquid B is 200 to 1000ppm. The health-care drinking liquid can regulate the insulin signaling channel in vitro level and improve the resistance of insulin so as to prevent the metabolic syndrome. The health-care drinking liquid prepared from the deep seawater has the advantages of rich resources, easiness in industrialization and the like, and has broad market and application prospect on the aspect of preventing and treating the metabolic syndrome.
WO2010056919A3 Eflornithine prodrugs, conjugates and salts, and methods of use thereof In one aspect, the present invention provides a composition of a covalent conjugate of an eflornithine analog with an anti-inflammatory drug. In another aspect, the present invention provides a composition of an eflornithine prodrug. In another aspect, the present invention provides a composition of an eflornithine or its derivatives aspirin salt. In another aspect, the present invention provides methods for treating or preventing cancer using the conjugates or salts of eflornithine analogs or eflornithine prodrugs.
US20090076026 Bronchodilators; treating chronic obstructive pulmonary disease or asthma; long duration of action; reduced side effects of dry-mouth and constipation; biphenyl carbamate derivatives; biphenyl-2-ylcarbamic acid 1-(3-(3-[3-(4-hydroxybenzylamino)propyl]-2-oxoimidazolidin-1-yl)propyl)piperidin-4-yl ester The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
WO2006036507A1 4-(heteroaryl-methyl and substituted heteroaryl-methyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists Compounds of formula (I) where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of formula (I) are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of formula (I) which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.
CN101757612A Gama-interferon high-efficient injection liquid for chickens and preparation method thereof The invention discloses a recipe of gama-interferon high-efficient injection liquid and a preparation method thereof. The method firstly prepares polyethyleneglycol gama-interferon for improving the plasma half-life of the gama-interferon and maintaining the constant blood medicine concentraction. However, because the antivirus activity of the polyethyleneglycol gama-interferon is reduced through being compared with the interferon per se, curative effect enhancing agents with polyinosine as main ingredients are added into the injection liquid and special stabilizing agents are selected for improving the antivirus activity of the gama-interferon, and the clinical utilization rate of the gama-interferon can be effectively improved.
CN103689598A Sheep placenta and blackcurrant composition with beauty function and application of sheep placenta and blackcurrant composition The invention discloses a sheep placenta and blackcurrant composition with a beauty function, which comprises the following components in parts by weight: 130-180 parts of blackcurrant seed oil, 20-30 parts of gamma-linolenic acid, 10-20 parts of blackcurrant extract, 3-8 parts of anthocyanin, 1-3 parts of vitamin C, 1-5 parts of zinc-bearing compound, 4-8 parts of tocotrienol, 1-3 parts of lecithin and 60-100 parts of sheep placenta. The sheep placenta and blackcurrant composition can effectively improve a metabolic function of females and allows skin of the females to be bright. The sheep placenta and blackcurrant composition with the beauty function can be applied to the field of preparing drugs for treating metabolic syndromes.
CN102731571A Novel crystalline s-(-)-ornidazole phosphate disodium hydrate and application thereof The invention relates to a novel crystalline s-(-)-ornidazole phosphate disodium hydrate and an application thereof. The hydrate disclosed herein is mainly used for sensitive protists and treating anaerobic bacteria infection.
WO2013092574A1 Isothiazolopyridine-2-carboxamides and their use as pharmaceuticals The present invention relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
WO2014160521A1 Piperazine derivatives and their use as kit modulators Compounds having structural formula (I) : or a pharmaceutically acceptable salt or a tautomer thereof or having structural formula (III) : or a pharmaceutically acceptable salt or tautomer thereof useful for treating disorders related to Kit are described herein.
WO2012055090A1 Drink for supplementing energy and recovering from fatigue, prepaing method and utility thereof A drink for supplementing energy and recovering from fatigue containing glucose-6-phosphate, its preparing method and utility are disclosed herein. The method is as following: mixing glucose, ATP and MgCl2, catalysing by hexokinase, thus obtaining a solution containing glucose-6-phosphate.
CN102764231A Ophthalmic gel for treating herpes simplex viral keratitis and preparation method of ophthalmic gel The invention discloses an ophthalmic gel for treating herpes simplex viral keratitis. The ophthalmic gel comprises five raw and auxiliary materials of ganciclovir, honeys, a mixture of polyethylene glycol 400 and polyethylene glycol 4000 and polysorbate 80. The ophthalmic gel is prepared by using new technologies of modern preparations and has stronger anti-herpes simplex viral actions and more obvious pesticide effects of promoting healing, repairing and regenerating of cornea than similar products, and the ophthalmic gel is safe for patients to take during usage.
CN1742726A Piperazine ferulate oral cavity disintegrating tablet and preparing method The present invention relates to a ferulic acid piperazine oral disintegrant tablet for curing nephritis, chronic nephritis, nephrotic synhrome and early uremia and auxiliary therapy of coronary heart disease, cerebral infarction and angitis, etc. and its preparation method. It is made up by using ferulic acid piperazine as main raw material and adding a certain auxiliary material through a certain preparation process.
WO2006094674A1 Nmda receptor antagonists in the medical intervention of metabolic disorders The present invention provides for the use of an NMDA receptor antagonist, preferably memantine or neramexane or a pharmaceutical acceptable salt or a prodrug of said antagonists, in the preparation of a pharmaceutical composition for the prevention, amelioration and/or treatment of disorders of metabolism influencing body weight, in particular obesity, an eating disorder and/or in the regulation of appetite. Furthermore, the present invention provides for a method for the prevention, amelioration and/or treatment of disorders of metabolism influencing body weight, in particular obesity, an eating disorder and/or in the regulation of appetite comprising the step of administering to a subject in need thereof a therapeutically effective amount of an NMDA receptor antagonist, preferably memantine or neramexane or a pharmaceutically acceptable salt or prodrug of said antagonists.
US20080108674 Comprising a micellular complex consisting of a cationic excipient, an anionic dye and a cationic antiseptic Aqueous antiseptic solutions and compatible dyes and methods for making and using such solutions are provided. Specifically, in one embodiment, the present invention relates to an antiseptic solution comprising a micellular complex consisting of a cationic excipient and an anionic dye. The antiseptic solution further includes a cationic antiseptic.
CN101721359A Potassium dehydroandrogrpholide succinate injection and preparation method thereof The invention discloses a potassium dehydroandrogrpholide succinate injection which contains the following components in 2,000ml of injection: 40.0g of potassium dehydroandrogrpholide succinate, 7.6g of sodium hydrogen carbonate, 7.0g of sodium dihydrogen phosphate anhydrous, 2.8g of disodium hydrogen phosphate, 2.8g of Beta-mercaptoethanol, 2.0g of medicinal carbon and the balance of injection water. A preparation method comprises the following steps of: after dissolving the sodium hydrogen carbonate by using the injection water with 50-60 DEG C, adding the potassium dehydroandrogrpholide succinate, stirring until the potassium dehydroandrogrpholide succinate is dissolved completely; and sequentially adding buffer solutions of the sodium dihydrogen phosphate anhydrous and the disodium hydrogen phosphate and the Beta-mercaptoethanol, uniformly stirring for constant volume, adding the active carbon for absorption, decarburizing and filtering, nitrogenizing and encapsulating after detecting that the semi-finished product is qualified, wherein the filling quality of the injection is 2ml. The preparation method is characterized in that: 1, a hollow fiber ultrafiltration device is used for replacing the original active carbon absorbed filtering system during the production; and 2, the quality of the semi-finished product of the potassium dehydroandrogrpholide succinate injection is controlled by using a high performance liquid chromatography.
US6861446 C7 heterosubstituted acetate taxane compositions Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
US20120141591 Drug Delivery Nanocarriers Targeted by Landscape Phage A targeted drug delivery nanocarrier and a method of forming the same is disclosed herein. The targeted drug delivery nanocarrier includes a plurality of amphipathic molecules forming a carrier particle having a plurality of drug molecules contained therein. A targeted landscape phage protein assembly is complexed to the carrier particle preferably using the unique method disclosed herein. The targeted landscape phage protein assembly displays a binding peptide that is selected to specifically and selectively bind to a target site. The method for forming targeted drug delivery nanocarriers includes the steps of obtaining a plurality of bacteriophage displaying a binding peptide for a desired target site, treating the bacteriophage with a denaturing agent, mixing the treated bacteriophage with a plurality of carrier particles and purifying the mixture to obtain a plurality of targeted drug delivery nanocarriers.
CN103565761A Galanthamine hydrobromide orally disintegrating tablet The invention provides a galanthamine hydrobromide orally disintegrating tablet, which has the characteristics of simple prescription, simple process, low cost and wide application, etc.
US20100003317 Compositions and methods for mediating rnai in vivo This invention relates to new formulated lipid particles (FLiPs) comprising at least one of a single or double stranded oligonucleotide, where the oligonucleotide has been conjugated to a lipophile and at least one of an emulsion or liposome to which the conjugated oligonucleotide has been aggregated, admixed or associated. These particles have surprisingly been shown to effectively deliver oligonucleotides to heart, lung and muscle where they effect gene silencing.
WO2012057312A1 Tau imaging probe One of the purposes of the present invention is to provide a probe for imaging a protein having a β-sheet structure for the purpose of diagnosing conformation diseases, particularly diseases in which the accumulation of tau protein in the brain is observed as the main characteristic symptom (tauopathy) such a Alzheimer's disease. Another one of the purposes of the present invention is to provide a compound which has high specificity to tau, enables the imaging of tau with good sensitivity, has high brain migration properties, is accumulated in bones in a minute amount or is not accumulated in bones, and has low toxicity or does not have toxicity. The present invention achieves the above-mentioned purposes by providing a compound represented by formula (I) (wherein A, R1, R2, R3 and others are as defined in the description) or a pharmaceutically acceptable salt or solvate thereof.
CN201831370U Electric heating health-care bed The utility model discloses an electric heating health-care bed, which has the technical scheme that a plurality of heating wires (2) are arranged on a bed baseboard (1), a heating tube (3) is respectively sleeved outside each heating wire, and the two ends of the adjacent two heating wires are connected through wires (4 and 5), and are then connected with a power supply plug (6) through wires (7 and 17). According to the utility model, a user can lie or lie on the stomach on the health-care bed, and the bed can dispel the cold of the whole human body after being heated. The utility model has the advantages that: (1) the bed is comfortable and convenient, and has an obvious effect; (2) the bed has a simple structure, and is easy to manufacture; and (3) the bed is economic and practical, and can be used in both hospitals and homes.
CN101437831A Ruthenium (II) compounds The present invention relates to a ruthenium (II) compound of formula (I) wherein X is halo or a neutral or negatively charged O, N- or S- donor ligand; Y is a counterion; m is 0 or 1; q is 1, 2 or 3; A is either: (i) (-NRR-R-<(N)>, where R and R are independently selected from H, optionally substituted C1-7alkyl, C3-20 heterocyclyl and C5-20aryl, and R is C1-2alkylene; or (ii) a nitrogen-containing C5-6aromatic ring, wherein the nitrogen ring atom is bound to the ruthenium atom, and the ring is also bound to the azo-nitrogen, either by a single bond wherein the bond is Alpha or Beta to the nitrogen ring atom, or to an axo-nitrogen atom by Alpha -CH2-base of nitrogen ring atom Alpha position; B is optional substituted C1-7alkyl, C3-20 heterocyclyl or C5-20aryl.
CN102716070A Pinocembrin and cyclodextrin or cyclodextrin derivative clathrate compound The invention discloses a pinocembrin and cyclodextrin or cyclodextrin derivative clathrate compound. Cyclodextrin or cyclodextrin derivatives are used for realizing the clathration on pinocembrin, the clathrate compound comprises the pinocembrin and cyclodextrin or cyclodextrin derivatives according to a mol ratio being 1:(1-100). The water solubility of the pinocembrin is improved, the treatment effect of the pinocembrin is more perfectly realized, the clathrate compound is suitable for being used for preparing solid preparations and liquid preparations required in clinics, and the preparations include transfusion, water injection, powder injection, oral liquid, syrup, tablets, capsules, granules and dispersible tablets. The clathrate compound can be used for preparing medicine for preventing and/or treating cardiovascular and cerebrovascular diseases, particularly cerebral apoplexy, and can also be used for preparing medicine for preventing and/or treating germ and/or fungal infection.
CN103040731A Preparation method of injection capable of improving body immunity The invention discloses a preparation method of injection capable of improving body immunity, and aims at solving the problems that the existing intramuscular injection produces precipitate when placed for a long time due to multi-component lentinan so that the product quality is influence, and the product cannot be used continuously. The method comprises the following steps of dissolving single lentinan or multi-component lentinan in 0.5-1.0mol/L HCl solution; stirring, and adding 0.1-0.6mol/L NaOH under the stirring condition to regulate the pH value to be between 6.5 and 6.8; filtering, and subpackaging required amount of filtrate into an ampoule; and sterilizing at a high temperature to obtain the product. According to the characteristic of stable aqueous liquid of lentinan and property of small dissolubility in water of lentinan, a method by which the dissolubility of lentinan is increased in water and product cannot produce precipitate after long-time placement can be discovered, and is used for preparing a lentinan water injection form.
US7507739 Against tumors expressing multiple drug resistance by promoting microtubule polymerization; deesterification of a phenyldiester with 3-amino-1,2,4-triazole, halogenation with a phosphorusoxyhalide, amination with a perfluoroalkylamine in the presence of a strong base and aprotic solvent This invention relates to certain 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof. The present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.
CA2296018C Inhibition of hiv-1 replication using oligocarbamate derivatives Tat-inhibitory oligocarbamate derivatives of the formula I (see formula I) and analogs thereof, and the biologically and pharmaceutically acceptable salts thereof exhibit advantageous properties, including specific binding to TAR RNA with high affinities, and stability of the resultant oligocarbamate-RNA complexes to proteolytic digestion. Site-specific photocrosslinking experiments using a photoactive analog (4-thio-uracil) containing TAR RNA indicate that these oligocarbamates interact with RNA in the major groove. These oligocarbamates are thus capable of competing with the TAR RNA-binding domain of Tat protein and thus are useful as a therapeutic agents in the treatment of AIDS.
EP1681292A1 3-Amino-6-aryl(or 6-heteroaryl)-thieno¬2,3-b|pyridin-2-carboxylic acid amides, pharmaceutical compositions comprising the said and their use as inhibitors of TNFalpha release 3-Amino-6-(hetero)aryl-thieno[2,3-b]pyridin-2-carboxylic acid amide (I) and their solvates, salts, prodrugs formulations, active metabolites or tautomers are new. 3-Amino-6-(hetero)aryl-thieno[2,3-b]pyridin-2-carboxylic acid amide of formula (I) and their solvates, salts, prodrugs formulations, active metabolites or tautomers are new. R1>1-naphthyl, 2-naphthyl, 1-anthryl, 2-anthryl, 1,2,3,4-tetrahydronaphth-5-yl, 1,2,3,4-tetrahydronaphth-6-yl (all optionally substituted with R3>), phenyl, 4-R3>-phenyl, 3-R3>-phenyl, 2-R3>-phenyl, 2-R3>,3-R3>-phenyl, 2-R3>,4R3>-phenyl, mono- or bicyclic 5-14C heterocyclic ring with 1-4 heteroatoms of N, O, S or Se, optionally substituted with R3>; R2>H, OH, 1-3C alkyl, 1-3C alkoxy, 1-3C alkylthio, 1-3C hydroxyalkyl, 1-3C mercaptoalkyl, cyclopropyl, 2-hydroxycyclopropyl, CH2F, CHF2, CF3, CH2Br, CHBr2, CBr3, CH2Cl, CHCl2, CCl3, CHFCH3, CF2CH3, CH2OAlk, CH2SAlk, CH2S(O)Alk, CH2S(O)2Alk, CH(OAlk)2 or CH(SAlk)2 (where Alk is 1-3C atoms); either R3>1-4C alkyl, 1-4C alkoxy, benzyl, benzyloxy (optionally substituted with R4>), trifluoromethoxy, difluoromethoxy, fluoromethoxy, 3-7C cycloalkyl, 3-7-cycloalkenyl, 3-7-cycloalkoxy, alkylthio, alkylsulfinyl, alkyl sulfonyl (where the alkyl is 1-4C), phenyl, 4-R4>-phenyl, 3-R4>-phenyl, 2-R4>-phenyl, 2-R4>,3-R4>-phenyl, 2-R4>, 4-R4>-phenyl, 2-R4>,5-R4>-phenyl, 2-R4>, 6-R4>-phenyl, 3-R4>, 4-R4>-phenyl, 3-R4>, 4-R4>, 5-R-4-phenyl, phenoxy, 4-R4>-phenoxy, 3-R4>-phenoxy, 2-R4>-phenoxy, 2-R4>, 3-R4>-phenoxy, 2-R4>, 4-R4>-phenoxy, 2-R4>, 5-R4>-phenoxy, 2-R4>, 6-R4>-phenoxy, 3-R4>, 4-R4>-phenoxy, 3-R4>, 4-R4>, 5-R4>-phenoxy, pyrid-2-yl, pyrid-3-yl, pyrid-4-yl, thien-2-yl, fur-2-yl, imidazol-2-yl, oxazol-2-yl, isoxazol-2-yl, pyrrazol-4-yl, 1-7C alkacyl (optionally substituted with R4>), formyl, benzoyl, 1- or 2-naphthoyl (optionally substituted with R4>), F, Cl, Br, I, NO2, OH, sulfhydryl, CN, rhodano, carboxyl, 1-4C alkoxycarbonyl, CONH2, CONHAlk, CONAlk2 (where Alk is 1-6C), SO3H, SO2OAlk, SO2NHAlk, SO2NAlk2 (where Alk is 1-5C), 1-6C alkylamino, di(1-5C)alkylamino, (thio)morpholino, thiomorpholino-S,S-dioxide, pyrrolidin-1-yl, piperidin-1-yl, piperazin-1-yl, 4-methyl-piperazin-1-yl, 4-hydroxyethyl-1-piperazin-1-yl, 4-phenyl-piperazin-1-yl, cycloalkylamino, 3-14C arylamino, heteroarylamino (e.g. phenyl, 1 or 2-naphthyl, 2, 3 or 4-pyridyl, chinolinyl, isochinolinyl, acridinyl, phenothiazinyl, 2-thienyl or 2-furylamino) (optionally substituted with carbo- and/or hetero-cyclic rings with R4>); or R3>+4-R3>OCH2O, OCH2CH2O, SCH2S or SCH2CH2S; and R4>1-4C alkyl, 1-4C alkoxy, trifluormethoxy, difluormethoxy, fluoromethoxy, alkylthio, alkylsulfinyl, alkyl sulfonyl (where alkyl is 1-4C), F, Cl, Br, I, NO2, OH, sulfhydryl, CN, rhodano, carboxyl, 1-4C alkoxycarbonyl, CONH2, CONHAlk, CONAlk2 (where Alk is 1-6C), SO3H, SO2OAlk, SO2NHAlk, SO2NAlk2 (where Alk is 1-5C), amino, 1-6C alkylamino or di(1-5C) alkylamino. Provided that (I) is not: when R1> is phenyl then R2> is CH3; when R1> is 4-bromo-phenyl then R2> is CH3; when R1> is 4-fluoro-phenyl then R2> is CH3; when R1> is 4-chloro-phenyl then R2> is H; when R1> is 4-methoxy-phenyl then R2> is CH3; when R1> is 3,4-dimethoxy-phenyl then R2> is CH3; and when R1> is thien-2-yl then R2> is CF3. An independent claim is also included for a composition (A) comprising (I), auxiliary materials and/or carriers. [Image] - ACTIVITY : Antiarthritic; Antirheumatic; Osteopathic; Antiasthmatic; Respiratory-Gen.; Immunosuppressive; Dermatological; Antiinflammatory; Antiulcer; Gastrointestinal-Gen.; Neuroprotective; Antipsoriatic; Nootropic; Antidiabetic; Antibacterial; Antimalarial; Cerebroprotective; CNS-Gen.; Nephrotropic; Antimicrobial; Analgesic; Antiarteriosclerotic; Cardiant; Vasotropic; Endocrine-Gen.; Vasotropic, Antiinflammatory; Ophthalmological; Cardiovascular-Gen.; Virucide; Cytostatic; Antiallergic; Muscular-Gen. - MECHANISM OF ACTION : Tumor necrosis factor (TNF) alpha inhibitor. The ability of (I) to inhibit TNF-alpha was tested using biological assays. The results showed that the median effective conc
US8828959 Antisense oligonucleotides capable of inhibiting the formation of capillary tubes by endothelial cells A pharmaceutical composition that blocks angiogenesis comprising as active agent at least one substance selected from the group consisting of (i) a nucleic acid molecule of a gene coding for protein IRS-1, a complementary sequence or a fragment thereof and (ii) a molecule which inhibits expression of a nucleic acid molecule according to (i).
EP1307189B1 Use of hydroxyethylrutosides for treating symptoms of common cold, allergic rhinitis and infections relating to the respiratory tract The present invention relates to methods of treating conditions and/or symptoms related to common cold of the upper and/or lower respiratory tract and/or eyes. In particular the invention relates to the methods of treating conditions and/or symptoms related to common cold comprising administration of a flavonoid or administration of a flavonoid in combination with a metal. The invention furthermore describes compositions comprising a metal and a flavonoid useful for the treatment of conditions and/or symptoms relates to common cold.
US20090221700 Carisprodol Articles and Methods A method of using carisoprodol comprises informing a user that administration of carisoprodol in the presence of food decreases the Cmax for carisoprodol compared to administration in the absence of food. In one embodiment, informing comprises providing printed labeling instructions. Also included are articles comprising a carisoprodol formulation and prescribing information, and methods of manufacturing carisoprodol dosage forms. Included are measures intended to increase the safe use of narrow therapeutic medications with carisoprodol.
US7820714 Increased selectivity for sialic acid binding Ig-like lectins (Siglec); improving immune response dependent on B-cells The invention relates to Siglec inhibitors that have an increased affinity for the receptor molecule. The Siglec inhibitors provided by the invention are preferably selective of a given Siglec molecule. The invention further relates to a method for producing Siglec inhibitors and to a method for increasing the binding selectivity for a given Siglec molecule. The invention also relates to pharmaceutical compositions that contain the Siglec inhibitors and to medical indications for the Siglec inhibitors.
WO2013069404A1 Therapeutic agent for joint diseases The purpose of the present invention is to provide a therapeutic agent for joint diseases, which has an activity of preventing the destruction of articular cartilages and has a high therapeutic effect. According to the present invention, a therapeutic agent for joint diseases can be provided, which comprises cyclic phosphatidic acid or carbacyclic phosphatidic acid as an active ingredient.
US8110399 Isolating nestin-positive stem cells, expanding and translplanting into a patient to replace lost or damaged insulin secreting cells; differentiating pancreatic stem cells to obtain cells that produce insulin and other hormones Methods and compositions are described for the treatment of type I insulin-dependent diabetes mellitus and other conditions using newly identified stem cells that are capable of differentiation into a variety of pancreatic islet cells, including insulin-producing beta cells, as well as hepatocytes. Nestin and ABCG2 have been identified as molecular markers for pancreatic stem cells, while cytokeratin-19 serves as a marker for a distinct class of islet ductal cells. Methods are described whereby nestin and/or ABCG2-positive stem cells can be isolated from pancreatic islets and cultured to obtain further stem cells or pseudo-islet like structures. Methods for ex vivo differentiation of the pancreatic stem cells are disclosed. Methods are described whereby pancreatic stem cells can be isolated, expanded, and transplanted into a patient in need thereof, either allogeneically, isogeneically or xenogenically, to provide replacement for lost or damaged insulin-secreting cells or other cells.
CA2350425C Use of an insulin sensitiser for the treatment of type 2 diabetes mellitus A method for the treatment of Type 2 diabetes mellitus and conditions associated with diabetes mellitus, which method comprises the administration to a human or non-human mammal in need thereof, of an effective non-toxic amount of an insulin sensitiser so as to provide a plasma concentration of the insulin sensitiser of at least a threshold level (the "Threshold Plasma Concentration") from within the range of effective plasma levels of the insulin sensitiser, compositions for use in such method and methodology for determining plasma concentrations of active agent use in such methods.
US20100111981 Synthetic monodisperse hemozoin crystals preparation and uses thereof A synthetic monodisperse hemozoin crystals preparation, compositions and methods of preparation thereof, are described. Also described are uses thereof, including use as an adjuvant, use in an immunogenic or vaccine composition, use for enhancing or inducing immunogenicity, and corresponding prevention or treatment of disease or infection.
EP2191841A1 Antitumor combinations containing antibodies recognizing specifically CD38 and vincristine Pharmaceutical composition comprising an antibody specifically recognizing CD38 and vincristine.
CN101933926A Indolylmaleimde derivatives as PKC inhibitors This invention relates to PKC inhibitors which are able to selectively inhibit e.g. the [alpha], [beta] and optionally [theta], isoforms of PKC, and their use in particular in transplantation.
US6897317 For therapy of arteriosclerosis and dyslipidaemias The tetrahydroquinolines can be prepared by condensing appropriately substituted tetrahydroquinoline aldehydes with suitable substances and subsequently varying the substituents present by customary methods. The tetrahydroquinolines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosis and dyslipidaemias.
EP1889831A2 Diazenedicarboxamides as inhibitors of D-alanine: D-alanine ligase (Ddl) This invention belongs to the field of pharmaceutical chemistry and relates to new diazenedicarboxamides as inhibitors of D-alanine:D-alanine ligaze (Ddl), to procedures for their preparation and pharmaceutical preparations containing the same. Compounds of general formula I: and the pharmaceutically acceptable salts are described. The appropriate substituents are clearly presented in the body of the text and in claims.
CN101824040A Active ingredient of psoralen and preparation method thereof The invention discloses an active ingredient of a natural medicament and a preparation method thereof. The active ingredient is characterized in that: the psoralen content is 90 to 97 percent; the active ingredient contains two impurities; and the impurity corylifolinin content is 3 to 8 percent, and the impurity bakuchiol content is less than 1 percent. Preferably, the psoralen content is 95 to 97 percent; the impurity corylifolinin content is 3 to 4.5 percent, and the impurity bakuchiol content is less than 0.5 percent. More preferably, the psoralen content is 96 to 97 percent; the impurity corylifolinin content is 3 to 4 percent, and the impurity bakuchiol content is less than 0.1 percent. Pharmacological experiments prove that the active ingredient has excellent effect of treating male erectile dysfunction.
US20110086096 Modified release 1- [ (3-hydroxy-adamant-1-ylamino)-acetyl] -pyrrolidine-2 (s) -carbonitrile formulation The subject invention provides a pharmaceutical tablet formulation comprising per unit dosage form e.g. per tablet the following ingredients: (a) a compound as an active ingredient, wherein the compound has a formula: [wherein R is substituted adamantly and n is an integer from 0 to 3 or a pharmaceutically acceptable salt thereof; (b) a hydroxypropyl methylcellulose with an apparent viscosity of 80,000 cP to 120,000 cP (nominal value 100,000 cP) when present in a 1% solution; (c) a microcrystalline cellulose; and (d) a magnesium stearate
US20110250193 Composition comprising expression or activity inhibitors of ninjurin1 for the prevention and treatment of inflammatory disease The present invention relates to a composition comprising a Ninjurin1 expression or activity inhibitor for the prevention and treatment of inflammatory disease. Ninjurin1 protein is specifically expressed in macrophages around blood vessels, increases cell-cell adhesion and cell-matrix adhesion, increases expressions of Wnt7b (Wingless-type MMTV integration site family, member 7B) and Ang2 (angiopoietin-2), but reduces expression of Ang1 to induce apoptosis of vascular endothelial cells. In addition, Ninjurin1 protein is up-regulated when inflammation is induced and induces iNOS expression as well as increased NO generation. Therefore, the Ninjurin1 protein expression or activation inhibitor can be effectively used as an active ingredient of a composition for the prevention and treatment of inflammatory disease.
WO2014040073A1 C13-hydroxy derivatives of oleanolic acid and methods of use thereof Disclosed herein are novel C13-hydroxy derivatives of oleanolic acid, including those of the formula (I): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
US7479499 Methods of using thalidomide in combination with irinotecan This invention relates to compositions comprising thalidomide and irinotecan, which can be used in the treatment or prevention of colorectal cancer. The invention also relates to methods of treating or preventing colorectal cancer which comprise the administration of thalidomide and irinotecan to a patient in need of such treatment or prevention. The invention further relates to methods of reducing or avoiding adverse side effects associated with the administration of irinotecan which comprise the administration of thalidomide to a patient in need of such reduction or avoidance.
CN102961330A Preparation technology of carbazochrome sodium sulfonate for injection The invention discloses a preparation technology of carbazochrome sodium sulfonate for injection, solving the shortcoming of the conventional preparation technology of carbazochrome sodium sulfonate injection. The preparation technology is low in cost, high in yield, and high in stability of the quality of carbazochrome sodium sulfonate. The preparation technology comprises the following steps of: (1) adding mannitol to about 25% of infusion water based on preparation amount, heating to completely dissolve, then adding 0.2% (W/V) medical carbon based on the preparation amount, boiling for 30 minutes, and decarburizing and filtering; (2) getting 30% of injection water based on the preparation amount, cooling to reach temperature less than 40 DEG C, adding absolute carbazochrome sodium sulfonate, stirring to completely dissolve, and adding the solution to the mannitol filtrate to uniformly mix; and (3) adjusting the pH (Potential of Hydrogen) of the liquid medicine into 5.5 to 6.0 by 10% of sodium hydroxide solution, adding the injection water until reaching the preparation amount, stirring uniformly, rechecking the pH between 5.5 and 6.0, sequentially filtering by microfiltration membranes of 0.45 microns and 0.22 microns, delivering semi-finished products for inspection, and filling after passing the inspection. By adopting the preparation technology, the market competitiveness of the carbazochrome sodium sulfonate is improved, the convenience is provided for market sales of the carbazochrome sodium sulfonate, and the preparation technology is worthy for popularization.
WO2006110118A1 Cytoprotection preparation The inventive cytoprotection preparation is based on an organic acid and used for preventing and treating a hypoxy of different aetiology. Said preparation contains at least gluconic acid anions, in particular, in the content of a pure gluconic acid or a pure magnesium gluconate. In the preferred embodiment, the preparation is presented in the form of a diGAMK-MG-gluconate compound or a binary salt selected from a group consisting of a magnesium succinate-gluconate, magnesium ascorbate-gluconate, magnesium glycinate-gluconate and the mixtures thereof.
US20110135708 Dietary supplement - liquid filled gum A new chewing gum comprising a gum member, with a central core or cavity, and a core element located within the central core or cavity. The chewing gum also comprises a dietary supplement, which may be incorporated in the central core, the cavity, or both. The core element can be of a range of consistencies, from fluid to gel-like. Optionally, the gum member may comprise crystals. Additionally, the crystals may comprise a dietary supplement. The chewing gum may be encapsulated with a coating. Multiple dietary supplements, of different or of the same varieties, may be incorporated into the chewing gum.
WO2010142663A8 Unsaturated fatty acid monoesters and diesters on ascorbic acid and cosmetic uses thereof The present invention relates to a compound with the following general formula (I): in which: R1 is a hydrocarbon chain of an unsaturated fatty acid from C12 to C24 including at least one unsaturation; and R2 and R3 are, independently or simultaneously: a hydrogen or a C1-C3 alkyl or a phenyl; and R4: a hydrogen atom or COR1', where R1' is a hydrocarbon chain of an unsaturated fatty acid from C12 to C24 including at least one unsaturation, advantageously 1 to 6 and preferably 1 to 4.
WO2014082960A1 Dermatitis treatment A compound of formula (I) R-L-CO-X (I) (wherein R is a C10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO2, said hydrocarbon group comprising at least 4 non-conjugated double bonds; L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO wherein L comprises at least one heteroatom in the backbone of the linking group; and X is an electron withdrawing group) or a salt thereof for use in the treatment of dermatitis.
CN1579397A Total matrine and use of its preparation in zoopharmacy The invention relates to application of matridine in curing flow and animals' bacteria infection, the matridine is extracted from the soybean plants.
CN101474151B Alkannin microemulsion composition The invention discloses a microemulsion composition containing alkannin, which comprises alkannin or alkannin ramification, emulsifier, assistant emulsifier, oil and water. The composition can greatly improve the solubility of the alkannin.
US20120004262 Phenylcyclopropylamine derivatives and their medical use The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.
US20130064903 Rheumatiod arthritis cure A cause and cure for Rheumatiod Arthritis which includes the body becoming acid and retaining fluids as a means of diluting said acid. Calcium with adequate vitamin D for absorption neutralizes said acid and brings the body back in balance. In addition, an overabundance of the mineral potassium slows the removal of fluid from the body causing fluid to be retained and stored in the joints and soft tissues. Said storage of retained fluid is what causes the symptoms of rheumatoid arthritis and related illnesses and even fibromyalgia and headaches. Joints become swollen and prolonged inflammation results in joint deformity. Said abundance of potassium also causes an imbalance of other minerals in the body, especially sodium, resulting in dehydration. Water and balanced electrolytes must be added to correct the problem.
US20120009147 2'-fluoro substituted carba-nucleoside analogs for antiviral treatment Provided are select imidazo[1,2-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2′ position of the nucleoside sugar is substituted with halogen and carbon substituents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.
WO2005002569A1 Pellet preparation of ranitidine The present invention discloses a pellet preparation of ranitidine, which is characterized in the fact that the pellet preparation consists of a core and a coating layer, which is relatively coated by three different kinds of material. The pellet preparation could be further prepared into pellet capsules or pellet tablets. The obtained preparation displays low hygroscopicity, good stability, as well as rapid disintegration and release in stomach.
CN1615878A Linwzolid powder injection and preparing method Linezolid powder for injection is prepared with linezolid as main medicine component, and through adding at least one of dextran, mannitol and sorbic alcohol as stuffing; dissolving with at least one solvent of injection water, acetone and alcohol to prepare solution; decoloring with active carbon, filtering with microporous filtering film and freeze drying or decompression drying. The present invention has the features of advanced preparation process, high product stability, convenient transportation, safe use and high effect. Linezolid as one antibiotic with new chemical structure has bacteria acting target site different from that of available antibiotics and is used in drug resistance preventing treatment clinically.
EP2338485A1 Substituted 1,3-dioxoisoindolines as medicine Substituted 1,3-dioxoisoindoline compounds (I) and their racemic mixtures, enantiomers, diastereomers, mixture of enantiomers, diastereoisomers or a single enantiomer or diastereoisomer and/or their salts are new. Substituted 1,3-dioxoisoindoline compounds of formula (I) and their racemic mixtures, enantiomers, diastereomers, mixture of enantiomers, diastereoisomers or a single enantiomer or diastereoisomer and/or their salts are new. X : -C(=O)-NH-, -NH(C=O)- or aryl group of formula (a1); R1 : OR6 or NR6R7; R6-R9 : H, 1-10C-alkyl (optionally saturated, optionally branched, optionally substituted by one or more substituents), 3-10C-cycloalkyl or heterocyclyl (both optionally bridged by 1-8C-alkyl, optionally saturated, optionally substituted by one or more substituents) or (hetero)aryl (optionally substituted by one or more substituents and optionally bridged by 1-8C-alkyl), where the alkyl chain is optionally branched, optionally saturated and optionally substituted by one or more substituents; either R2-R5 : H, F, Cl, Br, I, OR8, SR8, C(=O)OR8, CN, CF 3, NO 2, NR8R9, 1-10C-alkyl (optionally saturated, optionally branched, optionally substituted by one or more substituents), 3-10C-cycloalkyl or heterocyclyl (both optionally bridged by 1-8C-alkyl, optionally saturated, optionally substituted by one or more substituents) or (hetero)aryl (optionally substituted by one or more substituents and optionally bridged by 1-8C-alkyl), where the alkyl chain is optionally branched, optionally saturated and optionally substituted by one or more substituents; or R4CR5 : C(=O)-NR10-C(=O)-; and R10 : 1-10C-alkyl (optionally saturated, optionally branched, optionally substituted by one or more substituents), 3-10C-cycloalkyl or heterocyclyl (both optionally bridged by 1-8C-alkyl, optionally saturated, optionally substituted by one or more substituents) or (hetero)aryl (optionally substituted by one or more substituents and optionally bridged by 1-8C-alkyl), where the alkyl chain is optionally branched, optionally saturated and optionally substituted by one or more substituents, where the alkyl-, heterocyclyl- and cycloalkyl-substituents are F, Cl, Br, I, NO 2, CN, =O, CF 3, 1-8C-alkyl, (hetero)aryl, 3-10C-cycloalkyl, heterocyclyl, C(=O)OH, C(=O)O-1-8C-alkyl, C(=O)O-3-10C-cycloalkyl, C(=O)O-(hetero)aryl, C(=O)NH 2, C(=O)NH-1-8C-alkyl, C(=O)NH-3-10C-cycloalkyl, C(=O)NH-(hetero)aryl, C(=O)N(1-8C-alkyl) 2, C(=O)N(3-10C-cycloalkyl) 2, C(=O)N((hetero)aryl) 2, C(=O)N(1-8C-alkyl)(3-10C-cycloalkyl), C(=O)N(1-8C-alkyl)((hetero)aryl), C(=O)N(3-10C-cycloalkyl)((hetero)a ryl), C(=O)N(aryl)(heteroaryl), OH, OCF 3, O-1-8C-alkyl, O-3-10C-cycloalkyl, O-(hetero)aryl, O-C(=O)-1-8C-alkyl, O-C(=O)-3-10C-cycloalkyl, O-C(=O)-(hetero)aryl, SH, SCF 3, S-1-8C-alkyl, S-3-10C-cycloalkyl, S-(hetero)aryl, NH 2, NH-1-8C-alkyl, NH-3-10C-cycloalkyl, NH-(hetero)aryl, N(1-8C-alkyl) 2, N(3-10C-cycloalkyl) 2, N((hetero)aryl) 2, N(1-8C-alkyl)(3-10C-cycloal kyl), N(1-8C-alkyl)((hetero)aryl), N(3-10C-cycloalkyl)((hetero)aryl), N(aryl)(heteroaryl), NH-C(=O)-1-8C-alkyl, NH-C(=O)-3-10C-cycloalkyl and NH-C(=O)-(hetero)aryl, and the (hetero)aryl substituents are F, Cl, Br, I, NO 2, CN, CF 3, 1-8C-alkyl, (hetero)aryl, 3-10C-cycloalkyl, heterocyclyl, C(=O)OH, C(=O)O-1-8C-alkyl, C(=O)O-3-10C-cycloalkyl, C(=O)O-(hetero)aryl, C(=O)NH 2, C(=O)NH-1-8C-alkyl, C(=O)NH-3-10C-cycloalkyl, C(=O)NH-(hetero)aryl, C(=O)N(1-8C-alkyl) 2, C(=O)N(3-10C-cycloalkyl) 2, C(=O)N((hetero)aryl) 2, C(=O)N(1-8C-alkyl)(3-10C-cycloalkyl), C(=O)N(1-8C-alkyl)((hetero)ary l), C(=O)N(3-10C-cycloalkyl)((hetero)aryl), C(=O)N(aryl)(heteroaryl), OH, OCF 3, O-1-8C-alkyl, O-3-10C-cycloalkyl, O-(hetero)aryl, O-C(=O)-1-8C-alkyl, O-C(=O)-3-10C-cycloalkyl, O-C(=O)-(hetero)aryl, SH, SCF 3, S-1-8C-alkyl, S-3-10C-cycloalkyl, S-(hetero)aryl, NH 2, NH-1-8C-alkyl, NH-3-10C-cycloalkyl, NH-(hetero)aryl, N(1-8C-alkyl) 2, N(3-10C-cycloalkyl) 2, N((hetero)aryl) 2, N(1-8C-alkyl)(3-10C-cycloal kyl), N(1-8C-alkyl)((hetero)aryl), N(3-10C-cycloalkyl)((hetero)aryl), N(aryl)(heteroaryl), NH-C(=O)-1-8C-alkyl, NH-C(=O)-3-10C-cycloalkyl or NH-C(=O)-(hetero)aryl. [Image] [Image] - ACTIVITY : Analgesic; Antimigraine; Neuroprotective; Nootropic; Antiparkinsonian; Anticonvulsant; Eating-Disorders-Gen.; Anabolic; Anorectic; Ophthalmological; Neuroleptic; Antidiabetic; Antidepressant; Anesthetic; Antiemetic; Antiaddictive; Respiratory-Gen.; Laxative. - MECHANISM OF ACTION : Vesicular glutamate transporter 1 modulator; Vesicular glutamate transporter 2 modulator. The ability of (I) to inhibit vesicular glutamate transporter 1 was tested in rats. The results showed that 2-(4-(5-(2-carboxy-4-hydroxyphenylcarbamoyl)-1,3-dioxoisoindolin-2-yl )benzamido)-5-hydroxybenzoic acid exhibited an inhibitory activity of 98%.
EP1848448B1 Use of a bacterial lysate for the prevention of tuberculosis relapse Lyophilized bacterial extracts obtained by mechanical or alkaline lysis of bacteria responsible for infections of the upper and lower respiratory tract can be effectively used for the preparation of a medicament for the prevention of tuberculosis relapse, to be administered in association with antimicrobial agents.
CN102276612A C-2 substituted Aldisin derivative and medicinal salt thereof, their pharmaceutical composition, and application in preparation of antitumor drug thereof The invention discloses a C-2 substituted Aldisin derivative and medicinal salts thereof, their pharmaceutical compositions, and an application in preparation of antitumor drugs thereof. The C-2 substituted Aldisin derivative has a structure as shown in formula (I), wherein R represents phenyl, or phenyl which is mono-substituted by C1-C6 alkyl, C1-C6 alkoxyl, keto-carbonyl, amino, hydroxyl, hydroxymethyl, halogen, trifluoromethyl, cyano, or nitro at the ortho position, the meta position, or the para position, or phenyl which is substituted by 1'3-dioxygen bridged ring. The C-2 substituted Aldisin derivative and medicinal salts, pharmaceutical compositions thereof of the invention have certain inhibition effect on various tumor cells, and can be used to prepare drugs for treating tumors. More drug selection is provided for clinical treatment of tumors.
US20100069397 Sexual dysfunction compounds The present invention provides for a sexual dysfunction compound comprising a rapid-onset pharmaceutical composition that further comprises cocoa powder. The invention also provides for a process for manufacturing the composition, and use of the composition in sexual dysfunction therapy.
CN101978963A Annonaceous acetogenin extract, preparation method thereof and use thereof in cancer resistance and relief of cancerous pain The invention provides an annonaceous acetogenin extract extracted from seeds, leaves and barks of Annona squamosa L., a preparation method thereof, an external preparation taking the annonaceous acetogenin extract as an active ingredient, and medicinal use of the external preparation in cancer resistance and relief of cancerous pain. The preparation method for the annonaceous acetogenin extract has a simple process, common, low-price and low-toxicity reagents are adopted and are environment-friendly and relatively safe for human health, the production cost is lower, and the whole preparation method is easy to implement, can effectively shorten the production cycle and is suitable for mass production. An external patch comprising the annonaceous acetogenin extract serving as the active ingredient is easy to use, and has prominent curative effect on cancerous pain and no side effect.
CN102772428A Oral disinfectant antibacterial gargle The invention relates to an oral disinfectant antibacterial gargle. The purpose of the invention is to provide an oral disinfectant antibacterial gargle with characteristics of easy use, easy preparation, good stability and good taste; the gargle has antibacterial and disinfectant effects on oral pathogens to effectively prevent oral diseases. The technical solution provided by the invention is follows: the oral disinfectant antibacterial gargle is characterized in that the gargle has the following components in percentage by weight: 10-20 parts of boric acid; 0.5-1.1 parts of chlorhexidine or chlorhexidine acetate or chlorhexidine hydrochloride or chlorhexidine citrate or 3-5 parts of 20% chlorhexidine gluconate solution; 20-40 parts of glycerol; 1-3 parts of polysorbate 20; and the balance of purified water. The oral disinfectant antibacterial gargle provided by the invention is applicable to the oral disinfection for oral cavity, nasopharynx, and before and after periodontal surgeries.
CA2505487C Levobupivacaine and its use as an anaesthetic in obstetrics The present invention is directed to use of levobupivacaine or a salt thereof for use as an anaesthetic in obstetrics. In one embodiment, levobupivacaine is in at least 90% enantiomeric excess with respect to dexbupivacaine. Levobupivacaine is useful as an anaesthetic in a human patient having or disposed to depressed myocardial contractility.
CA2723561A1 Method of reducing side effects of non-steroidal anti-inflammatory drugs This invention relates to a method of reducing the side effects of non-steroidal anti-inflammatory drugs. Specifically, the invention relates to administration of a pyridine derivative to reduce and/or prevent the side effects of non-steroidal anti-inflammatory drugs. Also provided is the use of a pyridine derivative in the preparation of a medicament for the reduction of the side effects of non-steroidal anti-inflammatory drugs, and a pharmaceutical composition comprising a non-steroidal anti-inflammatory drug and a pyridine derivative.
EP1315481B1 Medicament for treating intestinal diseases The invention relates to a medicament for oral administration which releases its active substance substantially in the lower sections of the intestine. Said medicament consists of pellets, granules or minitablets that contain the active substance and that are individually coated with an enteric film. The medicament contains a mixture of two anionic copolymers of methacrylic acid and methyl methacrylate, the ratio of the free carboxylic groups to the methyl ester groups in the first copolymer being approximately 1:1 and in the second copolymer being approximately 1:2. The active substance used is for example 5-aminosalicylic acid or a pharmaceutically acceptable salt or pharmaceutically acceptable ester thereof, or a glucocorticoid.
DE102004015752A1 Treating or preventing renal diseases, especially renal ischemia, post ischemia and (re)perfusion disorders, using gabapentin lactam as cytoprotective preconditioning agent The use of gabapentin lactam (GBP-L) for the treatment and/or prophylaxis of renal diseases is new. - ACTIVITY : Nephrotropic; Vasotropic; Vulnerary; Antidiabetic; Cerebroprotective; Anticonvulsant; Neuroprotective. Freshly isolated isolated rat renal cortex tubular segments were pre-incubated (optionally in presence of tests agents) for 30 minutes in Krebs-Ringer-bicarbonate medium under 95% O2/5% CO2, incubated for 45 minutes under 95% N2/5% CO2 (anoxia) and reoxygenated in presence of 10 mM lactate under 95% O2/5% CO2 for 60 minutes (reperfusion). GBP-L 0.01-0.1 mM at showed a concentration-dependent cytoprotective effect, as evaluated by the increased intracellular potassium content, reduced loss of the marker enzymes lactate dehydrogenase (LDH) and glutamate dehydrogenase (GIDH), increased lactate gluconeogenesis, reduced release of oxygen radicals (as thiobarbituric acid reactive substances) and reduced indications of nuclear damage (by trypan blue staining). Typically in presence of 0.05 mM GBP-L the loss in LDH activity was reduced by 41% under N2 and by 16% under O2 and the loss in GIDH activity was reduced by 68% under N2 and by 64% under O2. - MECHANISM OF ACTION : None given.
CN103494837A Blood volume expanding pharmaceutical composition as well as preparation method and application thereof The invention discloses a blood volume expanding pharmaceutical composition as well as a preparation method and application thereof. The pharmaceutical composition comprises hydroxyethyl starch, sodium chloride, potassium chloride, calcium chloride, magnesium chloride, sodium acetate and the like. The pharmaceutical composition further can effectively maintain central body temperature of a patient while taking the fluid infusion effect, so that harms to a human body, such as increase of bleeding volume, increase of wound infection rate and delayed recovery caused by hypothermia are avoided.
CA2599295A1 Method of producing proanthocyanidin oligomer A composition containing, as the main component, a proanthocyanidin oligomer which is obtained by heating a plant material containing a proanthocyanidin polymer or its extract together with a substance having a phloroglucinol ring or resorcinol ring structure in an acidic solution, carries the substance having the fluoro/resorcinol ring structure attached thereto and has been degraded; a method of producing the same; and use of the composition in health foods, drugs and so on. Thus, the proanthocyanidin oligomer having a biological activity, carrying the substance having a phloroglucinol ring or resorcinol ring structure attached to the terminus thereof and having been degraded to a level allowing the absorption in vivo, which can be hardly obtained from a plant material at a high yield, can be efficiently and easily obtained.
US20100105757 Treatment and inhibition of disease conditions using flexible heteroarotinoids The present invention contemplates methods of treating, reducing, inhibiting or preventing several diseases by the administration of flexible heteroarotinoids. Among the diseases or conditions which can benefit from treatment with flexible heteroarotinoids as described herein are, (1) cancers and other diseases that involve abnormal differentiation, (2) diabetes, (3) hemophelia, (4) liver disease, (5) diseases involving human aldehyde dehydrogenase 2, (6) polycystic kidney disease, (7) lysosomal storage diseases, (8) high cholesterol, (9) obesity, (10) high triglycerides, (11) glycoprotein metabolism diseases, and (12) diseases involving abnormal angiogenesis.
US20050171162 Crystals of benzimidazole compounds Crystals of (S)-2[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or salts thereof, useful as excellent antiulcer drugs.
US20090047370 Topical treatment of peripheral neuropathy A method and composition for the treatment of diabetic neuropathy is disclosed. A preferred embodiment of the invention relates to a topical composition for the treatment of systems related to diabetic neuropathy by application to the affected area. The composition provides relief of these symptoms and inhibits those factors that contribute to these systems, such as an aldose reductase inhibitor A preferred embodiment of the invention relates to a method of treatment for diabetic neuropathy utilizing a regime of administrations of a topical composition in amounts effective to counter those areas of the body affected by peripheral neuropathy. Yet another preferred embodiment of the invention relates to a method of improvement of those areas effected by diabetic peripheral neuropathy using a topical composition over an effective period of time.
CN102775394A Amide compound, its preparation method and application The invention relates to an amide compound, preparation method and application. Specifically, the invention relates to compounds with a structure as shown in (I), their preparation methods and pharmaceutical compositions containing the compounds, as well as application in preparation of drugs treating and preventing mental diseases, wherein (C2-C3)n at least contains a carbon-carbon single bond and a carbon-carbon double bond, with the n being 8.
US20120095033 Selective Glycosidase Inhibitors and Uses Thereof The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
EP2451773A2 Novel polymorphic form of teriflunomide salts The present invention provides a new polymorph Form I of Teriflunomide sodium and a process for preparation thereof. The present invention provides an amorphous form of Teriflunomide sodium and a process for preparation thereof. The present invention provides a new polymorph Form I of Teriflunomide potassium and a process for preparation thereof. The present invention provides an amorphous form of Teriflunomide potassium and a process for preparation thereof. The present invention also provides particle size of Teriflunomide and its salts.
CN103040840A Treatment application of composition and product of composition The invention relates to an application of a composition in preparing a drug for treating infection, in particular to moderate or severe infection, and a product of the composition.
US20050266089 Contact lens and eye drop rewetter compositions and methods Stable ophthalmic formulations comprising hyaluronic acid (sodium hyaluronate) as the primary active demulcent ingredient, stabilized oxy-chloro complex (available commercially as OcuPure™ from Advanced Medical Optics, Purite® from Allergan, and Purogene from Biocide) for preservative efficacy, balanced salts mimicking the tear film, and sodium borate as a buffer are disclosed. In one embodiment, preferred stable formulations may be used in the human eye with or without contact lenses. In another embodiment preferred formulations may also be used as a storage and conditioning solution for contact lenses following disinfection.
US7157488 N-(2-(6-Fluoro-1H-indol-3-yl)ethyl)-3-(2,2,3,3-tetrafluoropropoxy)benzylamine; treating schizophrenia, anxiety, Alzheimer's disease, and cognitive disorders The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invention further provides a method of treating disorders associated with 5-HT6 receptors, including schizophrenia, anxiety, Alzheimer's disease, and cognitive disorders selected from the group consisting of age-related cognitive decline, mild cognitive impairment, and dementia, comprising: administering to a patient in need thereof an effective amount of a compound of formula I.
EP2413701A1 Sulfonyl-azetidin-3-yl-methylamine amide analogs as glyt1 inhibitors, methods for making same, and use of same in treating psychiatric disorders In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GIyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GIyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
DE102007043613A1 Medicament, useful for the treatment of Alzheimer's disease, comprises a pure biological alcohol, which is obtained from plants, preferably berries, fruits, herbs or its derivatives Medicament for treating Alzheimer's diseases, comprises a pure biological alcohol, which is obtained from plants, preferably berries, fruits, herbs or its derivatives, where the plants are grown in free of harmful environmental influences using natural fertilizers. An independent claim is included for treating Alzheimer's diseases comprising applying the biological alcohol to the body or drinking the biological alcohol, where 5-40% of alcohol is used for skin and 5-10% of alcohol in water used in eyes. - ACTIVITY : Neuroprotective; Nootropic. - MECHANISM OF ACTION : None given.
CA2550704C Nicotine transdermal delivery system The present invention provides a nicotine transdermal delivery system including an adhesive layer containing a free base nicotine and a liquid ingredient compatible with the adhesive, wherein the adhesive layer is crosslinked, and the liquid ingredient is contained in a proportion of 20-75 parts by weight, per 100 parts by weight of the adhesive layer as a whole. The nicotine transdermal delivery system has good adhesiveness and cohesion, and simultaneously achieves low irritation to the skin during peeling off and a fine feeling during adhesion.
WO2009098576A1 Pyridinyl amides for the treatment of cns and metabolic disorders The present invention relates to novel pyridinyl derivatives of Formula (I), wherein Y, Z, L, R1 through R11, n, m, p, q, t are as defined herein, that are 5-HT receptor ligands, particularly the 5-HT6 subtype, and as such are useful for treating diseases wherein modulation of 5-HT activity is desired. The present invention relates to novel pyridinyl derivatives including their pharmaceutically acceptable salts. The invention also relates to processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing and the uses of such compounds in treating diseases of the central nervous system such as schizophrenia.
US7071201 Serotonin antagonism; muscle relaxant for myotonia; such as 1-(1-(2-(4-methoxyphenyl)ethyl)piperidin-4-yl)-7-methoxy-1,2,3,4 -tetrahydroquinoline A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.
CA2610347A1 Alpha-carbolines as cdk-1 inhibitors The present invention embraces compounds of the general formula (I) in which R2 to R5 and X are as defined in Claim 1, these compounds being suitable for treating diseases characterized by excessive or abnormal cell proliferation, and also embraces their use for producing a medicinal product having the aforementioned properties.
US20090069390 Lennox-Gastaut syndrome and/or seizure disorders The present application describes deuterium-enriched rufinamide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN103110873A Ointment for treating chloasma faciei The invention discloses an ointment for treating chloasma faciei. The ointment comprises the following raw material ingredients by weight ratio: 48-52 of green persimmon leaf dry powder, 10-14 of radix angelicae dahuricae, 8-12 of coptis chinensis franch, 4-8 of rhizoma bletillae, 28-32 of aluminis usti, 6-10 of pyrolusite, 2-6 of rhizoma ligustici chuanxiong, 1-5 of camellia japomica, 6-10 of fructus tsaoko, 4-8 of short spike lagotis, 5-7 of herba houttuyniae, 1-5 of flos hibisci, 48-52 of Vaseline and 8-12 of resina liquidambaris. The recipe has the effects of clearing heat-fire, cooling blood and detoxifying; and the ointment has a good curative effect on treating chloasma faciei and does not have toxic or side effect.
CN102716173A Rapid anoxia-relieving capsule, preparation formula and preparation method thereof The invention discloses a novel rapid anoxia-relieving capsule, a preparation formula and a preparation method thereof. The rapid anoxia-relieving capsule employs biology enzyme technology, high and new fragmentation technology, and fine crushing technology, to extract effective essence in natural plants, according to a reasonable formula of a scientific proportion, a mixture is prepared. The rapid anoxia-relieving capsule is prepared thereby. The rapid anoxia-relieving capsule is prepared using the following active ingredients, sodium fructose diphosphate (FDP) with purity essentially more than 95 percent, rhodiola root powder with a crushing rate more than 90 percent, wall breaking mythic hungus spore powder with a wall breaking rate more than 99 percent. The capsule of the invention is extracted from green food essence, is nontoxic, harmless, has no obvious negative effect, has a small molecular weight, is easy to decompose and absorb, and is the rapid anoxia-relieving capsule that can relieve uncomfortable symptoms caused by anoxia rapidly.
CN101156843A A capsule for preventing and treating Alzheimer disease as well as its preparing method The invention relates to the biologic medicine field, and discloses capsule agent used to prevent and remedy alzheimer disease and the preparation technology thereof, in particular to capsule agent taking theanine as a main active component and a natural drug extract product as an auxiliary material. Along with the gradual increment of an elderly person, the alzheimer disease becomes a serious social problem and an important subject of the medicine field to be researched in 21 century in China. The product of the invention can effectively prevent and remedy the alzheimer disease, to ensure that the three major clinical symptoms of the alzheimer disease such as memory disturbance, cognitive function deficiency and dementia, etc. to be obviously improved. The theanine source is rich in China, the curative effect of the product of the technology is reliable, the price is cheap, the invention is adaptive to the National suitable, and the market foreground is wide.
CN101029043A Aspartic acid laumosaren hydrate, its production and use A hydrated lomefloxacin aspartate (C17H19F2N3O3.C4H7NO4.nH2O, where n=0.5-2.5) is an antibacterial fluoroquinolone medicine for treating the various infections of the gram-positive and gram-negative bacteria, and its preparing process are disclosed.
WO2013122303A1 Novel 2- aminothiazole derivative and anti-cancer composition comprising same as active ingredient The present invention relates to a novel 2-aminothiazole derivative, N-(5-(4-fluorophenyl)thiazole-2-il)-3-(furan-2-il)propane amide and to a use thereof as an anti-cancer drug. It is verified that the compound of the present invention has highly superior cancer cell-specific cytotoxic activity and in-vivo anti-cancer activity for inhibiting the growth of tumors in a animal model for cancer disease, and therefore can be developed as an anti-cancer candidate substance.
CN1974569A 8-octyl berberine hydrochloride and its synthesis process and application The present invention relates to one new kind of compound, named chemically as 8-octyl berberine salt (hydrochloride, bromide, iodide or hydrofluoride). The compound has the molecular expression of C28H34O4N .X, where, X is F-, Cl-, Br-, I- or other anion, and the structural formula as shown. Compound 8-octyl berberine salt has antibacterial activity, antilipemic activity and hypoglycemic activity obviously higher than that of berberine salt, and possesses excellent antibacterial, antilipemic and hypoglycemic medicinal value.
CN102836135A Aspirin enteric-coated tablet and preparation process thereof The invention provides an aspirin enteric-coated tablet and a preparation process thereof, belongs to the technical field of pharmaceutic preparations, and particularly relates to the aspirin enteric-coated tablet and the preparation process thereof. The invention provides the preparation process of the aspirin enteric-coated tablet, which dispenses with a granulation step, and the aspirin enteric-coated tablet with a low salicylic acid content, which is prepared through adopting the preparation process. Tablet cores of 1.5 millions of aspirin enteric-coated tablets provided by the invention comprise following components by weight ratio: 142.5Kg to 157.5Kg of aspirin, 15.39Kg to 17.01Kg of pregelatinized starch, 5.13Kg to 5.67Kg of starch and 8.55Kg to 9.45Kg of microcrystalline cellulose. The preparation process of the aspirin enteric-coated tablet provided by the invention comprises the following steps that (1) the aspirin, the pregelatinized starch, the starch and the microcrystalline cellulose are mixed; (2) a completely mixed material is tableted; (3) the tablet cores obtained after the tabletting are coated to obtain the coated tablets; and (4) the coated tablets are aired.
CN103446145A Application of Lycojaponicumin C in anti-tubercle bacillus drug The invention discloses application of Lycojaponicumin C in preparation of an anti-tubercle bacillus drug. Aiming at the situation that at present, the tuberculosis morbidity is high, multi-drug-resistant strains of mycobacterium tuberculosis are present and accordingly the tuberculosis morbidity and mortality are on the rise, we find that the Lycojaponicumin C has remarkable tubercle bacillus inhabiting activity and good application prospect. The application of the Lycojaponicumin C in the preparation of the anti-tubercle bacillus drug is disclosed for the first time. Due to the fact that the skeleton type is a novel skeleton type and the high tubercle bacillus inhabiting activity of the Lycojaponicumin C is previously unimagined, the possibility that other compounds give any revelation does not exist, and the Lycojaponicumin C has outstanding substantive characteristics and meanwhile has a remarkable improvement in prevention and curing of tubercle bacillus infection obviously.
WO2013130962A1 Benzofuran- 2 - sulfonamide derivatives as chemokine receptor modulators The present invention relates to novel benzofuran-2-sulfonamide pyridine derivatives of formula (1), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
CN101947225B Anticancer application of alkaloid The invention relates to an anticancer application of an alkaloid, in particular to an alkaloid, which provides an application of the alkaloid Exfoliazone in preparing medicines for treating cancers and an application of an orphan receptor Nur77 as an action target in screening marine organism resources. The invention is characterized in that the Exfoliazone can induce the apoptosis of cancer cells, the expression of the orphan receptor Nur77 and the nuclear export of the orphan receptor Nur77; the Exfoliazone induces the nuclear export transportation of the Nur77 through a CRM1 way and finally causes the apoptosis of liver cancer cells; the apoptosis effect of the Exfoliazone depends on the nuclear export of the Nur77; the Exfoliazone is taken as a regulatory factor targeted on the apoptosis way of the Nur77 and can become an effective medicine for treating the cancers; and the medicine for treating the cancers takes the orphan receptor Nur77 as the action target.
WO2006087230A1 Use of cdk ii inhibitors for fertility control The invention relates to the use of CDK II inhibitors of the general formulae (I) and (II) in the development of a contraception drug.
EP1507514A2 Controlled release compositions of estradiol metabolites The present invention provides improved sustained release formulations of estradiol metabolites, including 2-hydroxyestradiol, 2-methoxyestradiol, 4-hydroxyestradiol and 4-methoxyestradiol, useful for therapeutic treatments. The invention also provides methods of producing sustained release forms of estradiol metabolites. The compositions of the present invention include microparticles, nanoparticles, patches, crystals, gels, rods, stints, pellets, discs, lozenges, wafers, capsules, films, microcapsules, nanocapsules, hydrogels, liposomes, implants and vaginal rings. Compositions also include formulations for transdermal and intravenous delivery of estradiol metabolites. The present invention provides numerous improvements over previous forms of estradiol metabolites, such advantages including the sustained release of normally short half-life compounds to maintain therapeutic blood levels.
US7635673 Gene expression inhibition via contacting with tyrphostin; liposomes; drug screening The invention provides methods for inhibiting tumor cell proliferation by inhibiting FoxM1B activity, expression, or nuclear localization in a tumor cell. The invention also provides methods for preventing tumor progression in an animal comprising inhibiting FoxM1B activity, expression, or nuclear localization. Furthermore, the invention provides methods for inhibiting tumor cell growth in an animal comprising inhibiting FoxM1B activity, expression, or nuclear localization in tumor cells in the animal.
WO2005039581A1 Use of estrogen receptor ligands for the treatment of inflammatory bowel disease The present invention concerns a method of treating inflammatory bowel disease by diagnosing that a person is in need of treatment for inflammatory bowel disease and administering a therapeutically effective amount of a ligand which modulates NF-kB transcription factor by interaction with estrogen receptor ER-α, estrogen receptor ER-β, or both ER-α and ER-β estrogen receptors with a substantial absence of creatine kinase stimulation. In certain preferred embodiments, the administration is substantially without uterotropic activity.
WO2006114042A1 Application of levo-ornidazole in preparation of anti-anaerobic bacteria infection medicine An application of the levo-ornidazole in preparing the medicine for preventing and treating the anaerobe infection and the preparing process of said medicine is provided. A pharmaceutical preparation comprising levo-ornidazole as main active ingredient is also provided.
WO2010021385A1 Therapeutic agent for anca-related vasculitis Disclosed is an agent for preventing/treating ANCA-related vasculitis and/or preventing the recurrence of ANCA-related vasculitis. Also disclosed is a therapeutic method using the agent. Specifically disclosed is a pharmaceutical composition comprising at least one member selected from the group consisting of eicosapentaenoic acid, a pharmaceutically acceptable thereof and an ester thereof as an active ingredient. The pharmaceutical composition is useful for the prevention of recurrence of ANCA-related vasculitis, the treatment of chronic ANCA-related vasculitis, and the prevention and treatment of rapidly progressive glomerulonephritis (RPGN).
CN101721414B Composition containing pioglitazone hydrochloride and metformin hydrochloride and preparation thereof The invention provides a composition containing pioglitazone hydrochloride and metformin hydrochloride and preparation thereof. By controlling the particle diameter of about 80% of powder at 50-75mu m and the particle diameter of the rest powder below 50mu m by weight after the raw material of the pioglitazone hydrochloride is pulverized and selecting the recipe, the invention overcomes the low original dissolution rate of the pioglitazone hydrochloride in the original compound preparation and provides a compound pioglitazone hydrochloride and dimethyl biguanide preparation with higher original dissolution rate.
US7671053 such as 2-chloro-N-(1-hydroxy-cycloheptylmethyl)-5-[4-(2-hydroxy-3-methoxy-propyl)-3,5-dioxo-4,5-dihydro-3H-[1,2,4]triazin-2-yl]-benzamide for treatment of asthma and COPD; purinergic receptors (P2X7) The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
US7053082 Neuroprotectants for treating epilepsy, stroke, Parkinson's disease, multiple sclerosis or amyotropic lateral sclerosis; 5-(3-methyl-4-amino or nitro-phenyl)-1,3-dioxolo[4,5-h][2,3]benzodiazepine; AMPA/cainate antagonistic effect; chemical intermediates The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein R1 stands for methyl, formyl, carboxy, cyano, —CH═NOH, —CH═NNHCONH2 or —NR5R6, wherein R5 and R6 independently from each other represent hydrogen or lower alkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R2 is nitro or amino; R3 stands for hydrogen, lower alkanoyl or CO—NR7R8, wherein R7 and R8 independently from each other stand for hydrogen, lower alkoxy, lower alkyl or lower cycloalkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R4 is hydrogen or lower alkyl; the dotted lines have the following meaning: if R3 and R4 are not present, the bond between positions C8 and C9 is a single bond and the bond between positions C8 and N7 is a double bond; if R3 and R4 are present, the bonds between positions C8 and C9 and between position C8 and N7 are single bonds; and if R3 is present and R4 is missing, the bond between positions C8 and C9 is a double bond and the bond between positions C8 and N7 is a single bond) and salts thereof. The invention compounds have neuroprotective effect.
CN100575341C Tetrahydro-indolone derivative and tetrahydro-indazolone derivatives and their use A tetrahydroindolone derivative and its use are disclosed. It can inhibit malignant tumor cell growth. It can be used for mammary gland cancer, lung cancer, uterus neck cancer, rectum cancer, liver cancer and blood cancer.
US6852698 Free radical scavengers or promoters thereof as therapeutic adjuvants in preterm parturition The usage of compounds that improve fetal and neonatal outcome of preterm birth is described. These compounds are scavengers of ROS, their precursors, and agents that induce production of the scavengers. Examples of these compounds are glutathione, NAC, antioxidants, and spin trapping compounds. These compounds improve fetal outcome by inhibiting a fetal inflammatory process that may affect the fetus independently of prematurity. This fetal inflammatory response is characterized by increased cytokine and matrix metalloproteases (MMP) levels both in the mother and fetus and may be modulated by ROS at different levels. Targeting ROS formation with compounds such as specific antioxidants, glutathione or spin trapping compounds, their precursors, and/or agents which induce their production will suppress both the direct effects of ROS and its indirect effects through cytokines and MMPs already circulating in the system. This therapeutical intervention would limit the pathophysiologoical chain of events that ultimately leads to PPROM, preterm birth and/or adverse fetal and neonatal outcome.
CA2149776C Use of methioninase as an antitumor agent in anti-methionine chemotherapy The present invention describes methods for using methioninase as an antitumor reagent in anti-methionine chemotherapy. Specifically, methioninase is used to slow or stop cell division which can be enhanced with competitive inhibitors of methionine. In addition, methioninase can be used in combination with anti-mitotic agents to increase the therapeutic effectiveness of the antimitotic by inducing cell cycle synchronization.
EP2711011A1 Panaxadiol-containing composition A panaxadiol-containing composition, containing: panaxadiol; and at least one of sucrose fatty acid ester and lecithin.
EP1638540A2 Pyrazolidinedione derivatives and their use as platelet aggregation inhibitors Pyrazolidinedione derivatives of the general formula (I), wherein R1 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl or alkanoyl; and R2 is aryl or heteroaryl; tautomers thereof; geometric isomers thereof and tautomers of these geometric isomers, including mixtures of individual compounds of formula (I), or tautomers thereof, and their geometric isomers, or tautomers thereof, pharmaceutically acceptable acid addition salts of compounds which are basic; pharmaceutically acceptable salts of compounds containing acidic groups with bases; pharmaceutically acceptable esters of compounds containing hydroxy or carboxy groups; prodrugs of compounds in which a prodrug forming group is present; as well as hydrates or solvates thereof; are active as platelet adenosine diphosphate receptor antagonists and can be used for the prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, particularly thrombosis, and, respectively, for the manufacture of corresponding medicaments. Some, albeit not all, of the compounds of the above formula (I) are novel.
US20080269323 Use of 4-(nitrooxy)-butyl-(s)-2-(6-methoxy-2-naphthyl)-propanoate for treating pain and inflammation The present invention relates to the use of 4-(Nitrooxy)-butyl-(S)-2-(6-methoxy-2-naphthyl)-propanoate (naproxcinod) for treating pain and inflammation, in particular musculo-skeletal disorders, in patients with congestive heart failure, liver disease, cirrhosis, pre-existing renal disease, volume depletion, elderly with renal impairment, chronic renal failure or essential hypertension.
US20130058932 Use of pkc-iota inhibitors for the treatment of glioma The present invention pertains to use of PKC-iota inhibitors for treatment of glioma. In a specific embodiment, the treatment method comprises administering ICA-1 or a salt thereof to a subject with glioma. In another embodiment, the treatment method comprises contacting glioma cells with an effective amount of ICA-1 or a salt thereof.
US20120270864 2-quinolinone and 2-quinoxalinone-derivatives and their use as antibacterial agents The present invention relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation.
EP1805171A2 Indole acetic acids exhibiting crth2 receptor antagonism and uses thereof The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
DE202005012510U1 Topical composition for regenerating cartilage tissue or joint lubrication comprises emu oil, hyaluronic acid and vitamin K1 Topical composition for regenerating cartilage tissue or joint lubrication comprises at least 1 wt.% emu oil, at least 0.05 wt.% hyaluronic acid and at least 0.001 wt.% vitamin K1. - ACTIVITY : Antiarthritic; Antiinflammatory; Muscle relaxant. No biological data given. - MECHANISM OF ACTION : None given.
EP2505196A1 Antithrombotic agent An object of the present invention is to provide an antithrombotic agent that has fewer side effects and that is highly effective. The present invention provides an antithrombotic agent comprising (±)-[2-[4-(3-ethoxy-2-hydroxypropoxy)phenylcarbamoyl]ethyl]dimethylsulfonium p-toluenesulfonate represented by Formula (1) as an active ingredient.
CN1733312A Fluorouracil-dextran and process for preparing the same The invention provides a fluorouracil-dextran conjugate and its preparing process, which comprises, derivatizing fluorouracil, introducing acetic acid groups onto the N1 position of fluorouracil, carrying out esterification reaction by utilizing the hydroxyl on the carboxyl and the dextran, thus obtaining fluorouracil-dextran macromolecular precursor medicament.
CN101402640B Diester camptothecin derivative, preparation method and uses thereof The invention relates to a derivative of double-esterified camptothecin and the derivative has a structure as shown in the below general formula I, wherein, R1 represents polar group ((4-nitryl)-phenoxy) carbonyl or (4-(1-piperidyl)-1-piperidyl) carbonyl; R2 represents substituted or non-substituted hydrocarbons, substituted or non-substituted amines, substituted or non-substituted alcohols, substituted or non-substituted aromatics, cyanogens, nitryl, halogen, and the like. In addition, the invention also relates to a preparation method of the derivative of double-esterified camptothecin and the application of the derivative as well as salts and combinations of the derivative in the preparation of medicaments used for curing cell proliferation diseases, such as cancer and the like for the mammals.
US7091356 Tumor necrosis factor, to inhibit phosphodiesterase in a mammal Imido and Amido substituted alkanohydroxamic acids reduce the levels of TNFa and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.
EP1438073B1 Polyoxyalkylene conjugates as enzyme inhibitors The present invention relates to compositions which comprise one or more polymer conjugates having formula (I) wherein T is a heterocyclic unit which is capable of inhibiting one or more proteolytic enzymes; L is a linking group; [Poly] is a polymeric unit, i indicates the number of said heterocyclic units which comprise said conjugate and has the value of from 1 to 100; z is 0 or 1, said polymer conjugates suitable for use in preventing skin irritation resulting from exposure of the skin to body fluids, inter alia, faces, menstrual fluid. The conjugates of the present invention are useful in diapers, dressings, sanitary napkins, and the like.
WO2010020789A3 Medicament combination comprising alkaloids and a purine analog antiviral agent A medicament for treating neurally-transported viral infections, such as herpes simplex, herpes zoster or rabies, comprises a first active substance selected from alkaloids, anaesthetics and griseofulvin and a second active substance comprising a purine analogue or pyrimidine analogue antiviral agent. The alkaloid may comprise colchicine, vinblastine, vincristine, a cytochalasin or their derivatives. Suitable purine analogues include N- substituted guanine derivatives such as aciclovir, valaciclovir, penciclovir, famiciclovir ganciclovir, valganciclovir or pro-drugs that convert thereto in the body, and N-substituted adenine derivatives such as vindarabine. Suitable pyrimidine analogues include thymidine derivatives such as trifluorothymidine. The medicament may be orally administrable, injectable, infusible or topically applicable; a topical medicament may include a local anaesthetic. The medicament may be administered in response to a risk of infection, prior to onset of symptoms. A combination of two preparations may be used, respectively containing the first and second active substances, either administered sequentially or simultaneously.
CN103102332A Chalcone compound containing piperazine ring and preparation and application thereof The invention provides a type of chalcone compounds containing piperazine rings. The preparation method comprises the following steps: mixing fluoroacetophenone and N-methyl piperazine, heating and refluxing to prepare p-methyl piperazine acetophenone under the action of alkali, mixing with an aromatic aldehyde compound to prepare the chalcone compounds containing the piperazine ring. The pharmacological experiment proves that the compound has high inhibition effect on the human MCF-7 tumor cells and can be applied in the preparation of medicines for treating breast cancer. The compound is mild in preparation conditions, convenient to operate and low in cost and has wide industrial application prospect. The compound lays a foundation for screening and developing of new anti-breast cancer drugs and has high application value. The compound has the general formula.
US20090093521 2, 5-Bis-Diamine [1,4] Benzoquinone-Derivatives Synthesis of 2,5-bis-diamine-[1,4]benzoquinonic derivatives having the general formula (I), products and intermediates of said synthesis; the synthesis involves the use of p-benzoquinones having the general formula (IX) and diamines having the general formula (XI).
CN103202808A Method for preparing multi-functional gossypol nano preparation by using one-pot method The invention discloses a method for preparing a multi-functional gossypol nano preparation by using a one-pot method. The method comprises the following steps of: fully dissolving gossypol, ester fluorochrome and a polyethylene glycol derivative in certain proportions by using a certain amount of an organic solvent; dropwise adding a certain amount of a surfactant into a certain amount of deionized water; at an appropriate rotational speed, dropwise adding a mixed solution of the gossypol, the ester fluorochrome and the organic solvent into the deionized water at a certain dropwise adding speed; and after the dropwise adding process is completed, carrying out reaction for a certain time, and after the organic solvent is dried through rotating, obtaining the multi-functional gossypol nano preparation. The method disclosed by the invention is simple in preparation process, the prepared gossypol nano preparation has the advantages of small particle size, high drug loading capacity, good monodispersity and stability, traceability, high security, and the like, therefore, gossypol can play an anti-tumor role better.
CN102670525A Application of ursolic-acid nano medicine-carrying microspheres for treating tumors and preparation The invention relates to the application of ursolic-acid nano medicine-carrying microspheres for treating tumors. The ursolic-acid nano medicine-carrying microspheres contain ursolic acid and a medicine-carrying material which are mixed, wherein the medicine-carrying material is a biparental segmented copolymer synthesized by one of polycaprolactone, polylactic acid or polyglycolic acid and polyethylene glycol, i.e. polycaprolactone-polyethylene glycol (mPEG-PCL), polylactic acid-polyethylene glycol (mPEG-PLA) or polyglycolic acid-polyethylene glycol (mPEG-PLGA); and the ursolic-acid nano medicine-carrying microspheres comprise 5 to 35wt% of ursolic acid and 65 to 95wt% of medicine-carrying material which are mixed.
CA2446705C Compositions of quinoxaline-based therapeutic agents and fatty acids having enhanced pharmacokinetic characteristics Compositions comprising a therapeutic component and an efficacy enhancing component, that enhances the pharmacokinetic disposition of the therapeutic component, are disclosed. The therapeutic component may include an alpha-2-adrenergic agonist and the efficacy enhancing component may include fatty acids. In one embodiment, the therapeutic component and the efficacy enhancing component form a complex.
WO2014062143A3 Combinations of glycopyrrolate and an anticholinergic agent The present invention relates to pharmaceutical compositions comprising glycopyrrolate and an anticholinergic agent for use in treatment of asthma and chronic obstructive pulmonary disease (COPD).
US20120269831 Substituted pyrido[2,3-d]pyrimidin-7(8h)-ones and therapeutic uses thereof Compounds useful as antiproliferative agents according to Formula (I), wherein n, A, R1, R2, and Ar1 are as defined herein, and salts thereof; antibody conjugates, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.
US20120183585 Gel based wound dressing and a method of synthesizing the same The various embodiments herein provide a gel based wound dressing comprising a lyophilized powder and a water-based solvent. The lyophilized powder comprises several nanoparticles and water miscible natural or synthetic polymers. The nanoparticles comprises pectin and a wound healing agent or an anti-microbial agent. The anti-microbial agent is nisin. The lyophilized powder and the water-based solvent are kept in two separate sealed packages and are mixed together before applying on a wound. The embodiments herein also provide a method of synthesizing the gel based wound dressing. The nano-particles control a release of the wound healing agent or the antimicrobial agent to a wound.
CN101450947B 7-(3-oximido-4-amido-4-alkyl-1-piperidine)quinoline carboxylic acid derivates and preparation method thereof The invention provides 7-(3-oximido-4-amino-4-alkyl-1-piperidyl) quinoline carboxylic acid derivatives with excellent antibacterial activities, preparation methods thereof, antibacterial agents containing the compounds, and uses of the compounds as antibacterial agents and feed additives. A substituent of (3-oximido-4-amino-4-alkyl-1-piperidyl) is at a 7-position of a carbostyril nucleus. Compared with the prior fluoroquinolone antibacterial drugs, the antibacterial agents have more excellent anti-gram-positive-bacteria activities and broad-spectrum antibacterial activities.
US20090233992 Hepatitis c virus vaccine The present invention features Ad6 vectors and a nucleic acid encoding a Met-NS3-NS4A-NS4B-NS5A-NS5B polypeptide containing an inactive NS5B RNA-dependent RNA polymerase region. The nucleic acid is particularly useful as a component of an adenovector or DNA plasmid vaccine providing a broad range of antigens for generating an HCV specific cell mediated immune (CMI) response against HCV.
CN101181631B Compound prescription for preventing and improving osteosporosis as well as preparation method thereof The invention discloses a compound formulation used for preventing and improving osteoporosis, which is prepared by calcium citrate, calcium carbonate, magnesium citrate, zinc citrate, collagen, vitamin D3 and certain accessories through evenly mixing according the proportion of the formulation. The invention has high absorbing rate, which can be used for preventing and improving osteoporosis, maintaining normal physiological activities, thereby being suitable to be eaten as health-care food for a long time.
US20080044405 Noble metal complex-mediated immunosuppression Certain noble metal complexes are able to strip peptides from class II MHC proteins, resulting in class II MHC peptides in a peptide-empty conformation that do not support T-cell activation. Methods for identifying additional compounds are provided. Also provided are methods for use of this class of compounds to inhibit an immune response and to treat subjects having an unwanted immune response such as autoimmunity, allograft rejection, allergy, asthma, and inflammation.
WO2012136351A8 Tapentadol for treating pain associated with trigeminal neuralgia The invention relates to tapentadol for use in the treatment of pain associated with disorders of the trigeminal nerve, in particular for use in the treatment of pain associated with trigeminal neuralgia.
US8013126 84P2A9: a prostate and testis specific protein highly expressed in prostate cancer A novel gene (designated 84P2A9) and its encoded protein is described. While 84P2A9 exhibits prostate and testis specific expression in normal adult tissue, it is aberrantly expressed multiple cancers including prostate, testis, kidney, brain, bone, skin, ovarian, breast, pancreas, colon, lymphocytic and lung cancers. Consequently, 84P2A9 provides a diagnostic and/or therapeutic target for cancers, and the 84P2A9 gene or fragment thereof, or its encoded protein or a fragment thereof used to elicit an immune response.
US20120034292 Composition For Transdermal Delivery Of Fentanyl A transdermal drug delivery composition comprises an acrylate copolymer and from about 8% to about 30% by weight fentanyl. A transdermal fentanyl delivery composition comprising methyl laurate or tetraglycol as a permeation enhancer is also provided. The transdermal drug delivery compositions can be used to make a transdermal drug delivery device for the delivery of fentanyl.
CN1660067A Application of liganans of biphenyl cyelo-octadiene in preparing antineoplastic medicine An application of 1-hydroxy-2,3,12,13,14-pentamethoxy-6- hexanoately-7-hydroxy-8-methyl-9-benzoately-biphenyl cyclooctadiene lignan, white is extracted from schisandra propinqua, in preparing antineoplastic medicines is disclosed.
CN102614208A Application of compound (20R,24R)-24,25-16,23-23,27-triepoxy-12-acetoxyl-9,19-cyclolanostanol-3-O-beta-D xylopyranoside in pharmacy The invention relates to an application of a compound DA (20R,24R)-24,25-16,23-23,27-triepoxy-12-acetoxyl-9,19-cyclolanostanol-3-O-beta-D xylopyranoside extracted from cimicifugae foetidae in pharmacy, in particular to an application of the compound DA in preparation of medicines for resisting breast cancer as well as a preparation method for the compound DA.
WO2005025621A1 Methods and compositions for reducing the risk associated with the administration of opioid analgesics in patients with diagnosed or undiagnosed respiratory illness The present invention relates to methods for reducing the risk associated with the administration of opioid analgesics in patients diagnosed or undiagnosed with respiratory illness by administering an analgesic composition comprising a sub-analgesic dosage of a µ-opioid agonist selected from the group consisting of morphine, fentanyl, sufentanil, alfentanil, oxymorphone and hydromorphone, or a pharmaceutically acceptable salt thereof, and a sub-analgesic dosage of oxycodone which is a K2 -opioid agonist or a pharmaceutically acceptable salt thereof.
WO2012068032A1 Fgfr1 extracellular domain combination therapies Methods of treating cancer comprising administering a fibroblast growth factor receptor 1 (FGFR1) extracellular domain (ECD) and/or an FGFR1 ECD fusion molecule in combination with at least one additional therapeutic agent selected from docetaxel, paclitaxel, vincristine, carboplatin, cisplatin, oxaliplatin, doxorubicin, 5-fluorouracil (5-FU), leucovorin, pemetrexed, and bevacizumab are provided. Dosage packs comprising an FGFR1 ECD and/or an FGFR1 ECD fusion molecule and/or at least one additional therapeutic agent selected from docetaxel, paclitaxel, vincristine, carboplatin, cisplatin, oxaliplatin, doxorubicin, 5-fluorouracil (5-FU), leucovorin, pemetrexed, and bevacizumab are also provided. In some embodiments, a dosage pack comprises instructions for administering FGFR1 ECD and/or FGFR1 ECD fusion molecule with at least one additional therapeutic agent.
CA2157668C Tricyclic 2,3,4,5-tetrahydro-1h-3-benzazepines, their use and preparation Tricyclic benzazepines having general formula (I) wherein A together with the .alpha.- and .beta.-marked carbon atoms is a cyclopentene, cyclohexene, furan, dihydrofuran, pyran, dihydropyran, thiophene, oxazole, pyrrole pyrroline, tetrahydropyridine or dioxole ring, R1 is H or alkyl, R2 and R3 independently an H, alkoxy, halogen, nitro, cyano or hydroxy, or R2 and R3 together may form a furan, dihydrofuran, cyclopentene or dioxole ring and R4 is H, alkoxy, nitro, cyano, hydroxy or halogen, or a pharmaceutically acceptable salt thereof, are useful in treatment of certain disorders in the central nervous system, e.g., psychosis, pain, depression, sleep disturbances, dyskinesia, Parkinson's disease, stroke.
CN102784384A Application of combination of low-dose naltrexone and methionine-enkephalin to preparation of anti-cancer drug The invention relates to application of combination of low-dose naltrexone and methionine-enkephalin to preparation of an anti-cancer drug. The low-dose naltrexone and the methionine-enkephalin are combined via an opioid receptor on the surface of a cell of an immunity system of a body, so that effects of stimulating activation and proliferation of immune cells and improving an immune function can be realized. In addition, the combination of the low-dose naltrexone and the methionine-enkephalin is used for preparing the drug for treating cancers, so that a novel tumor biotherapy method with a breakthrough curative effect is formed, and the drug has the advantages of low dosage and side effect, high activity and safety, and the like.
US20050004217 Utilizing cistaceous plant extract; safe, side effect free; An accelerator of collagen production containing a compound represented by formula (I) or a salt thereof wherein the three dotted lines represent two single bonds and one double bond.
US20080139625 Metabolic syndrome; compounds are 1,3-substituted-2-oxo-(pyrrolidines or piperidines); 3-[(2,6-Dichlorophenyl)methyl]-1-(1-phenylpropyl)-2-pyrrolidinone for example Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl Or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.
US8119397 Therapeutic agents and therapeutic methods for treating injured tissue This invention provides therapeutic agents, transplants and therapeutic methods that can enhance the regeneration of injured tissue. This invention relates to agents, transplants and therapeutic methods for enhancing the migration and accumulation of mesenchymal stem cells in injured tissues and/or suppressing the diffusion of mesenchymal stem cells from injured tissues.
EP1658065A2 Using selective antagonists of persistent sodium current to treat neurological disorders and pain The present invention provides uses of compounds as medicaments for treating neurological disorders and chronic pain in mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current.
CN101204169A Strengthening nutritional additive powder with high dietary fiber The invention relates to a dietary fiber enriched powder, which pertains to the technological field in which flour is processed by adding organic substances. The invention is characterized in that the dietary fiber enriched powder is only added with polydextrose with high dissolubility as enriched nutrient component, and the addition amount of the polydextrose ranges from 10g/kg to 40g/kg. The flour of the invention has good taste and is not easy to lose fibrin.
CN101987091A Venlafaxine hydrochloride sustained-release pellet capsules The invention provides a novel venlafaxine hydrochloride sustained-release pellet capsules. Each capsule comprises a capsule shell and sustained-release pellets in the shell, wherein the capsule shell can be made from common gelatin capsule or other materials; each sustained-release pellet has a double-sustained-release structure with internal pellet core frame sustained-release and sustained-release coat, and the structure can realize better release characteristic and higher safety, wherein the sustained-release coat takes polyacrylic resin as a coating material and preferably takes aqueous dispersion coat of polyacrylic resin NE30D, and the pellet core preferably adopts polyacrylic resin NE30D which serves as frame sustained-release material, binder and wetting agent. The pellet core of the sustained-release pellet is prepared by an extrusion rounding method, preferably improved extrusion rounding method, namely an extruder with a circulation cooling device is adopted, wherein the temperature of the extruded product is controlled at 15-45 DEG C, and the water content of the extruded product is kept to be proper; and the thermal treatment of the coated sustained-release pellets is gradient warming thermal treatment.
WO2006103401A3 N-alkylcarbonyl-amino acid ester and n-alkylcarbonyl-amino lactone compounds and their use The present invention generally relates to refreshing, soothing, and cooling compounds that affect sensory processes. More particularly, the present invention pertains to certain N-alkylcarbonyl-amino acid ester and N-alkylcarbonyl-amino lactone compounds as described herein; compositions and articles comprising such compounds; and methods of treatment, for example, methods of alleviating the discomforts of irritation, itch, and pain in the skin and in the linings of the oral cavity and upper respiratory tract, for example, in methods of treatment of cough and/or asthma.
EP1142573B1 Pharmaceutical compositions comprising faropenem sodium and a diamineacetate compound for improving gastrointestinal absorption A technique of widely applying penem compounds to antibacterial medicinal compositions is developed. Antibacterial medicinal compositions containing penem compounds as the active ingredient which are characterized by containing α,φ-diamineacetic acid compounds.
CN103520262A Lipid soluble gynecological gel The invention discloses a lipid soluble gynecological gel. The lipid soluble gynecological gel is prepared from the following raw materials in parts by weight: 8-15 parts of L-ascorbic acid palmitate, 10-23 parts of fructus cnidii, 7-17 parts of radix sophorae flavescentis, 2-8 parts of borneol, and 2-6 parts of vitamin E. The lipid soluble gynecological gel has no hormone, no stimulation and no toxic and side effects, and is noninvasive. When being used for curing gynaecopathia, the lipid soluble gynecological gel can reconstruct the environment in the genital tract, regenerate effective microbial communities, eliminate the lipid soluble toxin in a body, improve self immunity, and is more convenient and safer in use.
EP0954340B1 Targeted combination immunotherapy of cancer The invention provides a method for effecting therapy of a tumor in a patient, comprising the steps of: (A) administering to the patient a first conjugate comprising a targeting moiety, a first member of a binding pair, and a first therapeutic agent, wherein the targeting moiety selectively binds to a marker substance produced by or associated with the tumor, and allowing the conjugate to localize at the tumor, thereby effecting therapy of the tumor; (B) optionally, administering to the patient a clearing composition, and allowing the clearing composition to clear non-localized first conjugate from circulation; (C) administering to the patient a second conjugate comprising a complementary member of the binding pair and a second therapeutic agent, wherein the second therapeutic agent is the same as or different from the first therapeutic agent, and allowing the second conjugate to localize at the tumor, thereby effecting therapy of the tumor.
CN103191072A Simvastatin tablets and preparation method thereof The invention discloses Simvastatin tablets and a preparation method thereof. The Simvastatin tablets are prepared by directly tabletting Simvastatin lipidosome clathrate compound and pharmaceutically acceptable auxiliary materials. The Simvastatin lipidosome clathrate compound is prepared by the following steps of: dissolving Simvastatin, hydroxypropyl betacvclodextrin and lecithin in absolute ethyl alcohol, and removing ethanol by drying under reduced pressure to obtain the Simvastatin tablets. No acid agent or antioxidant is added to the Simvastatin tablets disclosed by the invention, so that the side effects of the Simvastatin tablets are reduced, and meanwhile, the safety of the Simvastatin tablets is improved. Meanwhile, the stability of the tablets is good, the dissolution of the tablets is rapid, the preparation process is simple, and the tablets and the preparation method are suitable for industrialized mass production.
WO2010132777A2 Treatment of urinary tract infections with antibacterial aminoglycoside compounds A method for treating a urinary tract infection in a mammal in need thereof is disclosed, the method comprising administering to the mammal an effective amount of an antibacterial aminoglycoside compound.
WO2007058991A3 Mutations and polymorphisms of c-abl This invention relates generally to the analytical testing of tissue samples in vitro, and more particularly to aspects of genetic polymorphisms and mutations of the c ABL gene. The invention provides new c ABL mutations and SNPs, useful in the diagnosis and treatment of subjects in need thereof. Accordingly, the various aspects of the present invention relate to polynucleotides encoding the c ABL mutations of the invention, expression vectors encoding the c ABL mutant polypeptides of the invention and organisms that express the c ABL mutant and polymorphic polynucleotides and/or c ABL mutant/polymorphic polypeptides of the invention. The various aspects of the present invention further relate to diagnostic/theranostic methods and kits that use the c ABL mutations and polymorphisms of the invention to identify individuals predisposed to disease or to classify individuals with regard to drug responsiveness, side effects, or optimal drug dose.
WO2008090585A3 Soluble forms of inclusion complexes of histone deacetylase inhibitors and cyclodextrins, their preparation processes and uses in the pharmaceutical field The invention relates to the preparation of soluble forms of complexes of histone deacetylase inhibitors and cyclodextrins. The preparation process involves the formation of inclusion complexes with cyclodextrins with the aid of microwaves. Their use is in the pharmaceutical field.
WO2009053268A1 Novel phenyl-substituted piperazino-dihydrothienopyrimidines The invention relates to novel dihydrothienopyrimidines of the formula 1, and to pharmacologically acceptable salts thereof, formula (1) in which X is SO or SO2, but preferably SO, and either R3 is a monosubstituted phenyl ring in the ortho position or in the meta position, or R3 is a phenyl ring bisubstituted in any positions, and pharmaceutical compositions which comprise these compounds. These novel dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal symptoms or disorders, inflammatory disorders of the joints, of the skin or of the eyes, disorders of the peripheral or central nervous system or cancers.
US7160886 For therapy and prophylaxis of obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
WO2009024980A3 Pyrimidine and pyridine derivatives as posh and posh-ap inhibitors Pyridine and pyrimidine derivatives inhibit ubiquitination of human polypeptides, particularly of POSH and POSH-associated proteins such as HERPUD1, and can be used as medicaments for treatment of viral infections caused by virus such as HIV and for treatment of neurological disorders or diseases.
US20080161354 Stable s-nitrosothiols, method of synthesis and use The present invention relates to stable S-nitrosothiols derivatives of formula (I) having vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).
CN201524268U Extended release pills in micro-capsules The utility model discloses an extended release pill in micro-capsules, which includes an original medicament layer in complex phospho-esterase and a coating for the pill, and is characterized in the an extended release micro-capsule core layer is provided inside the original medicament layer in complex phosphor-esterase. Using the extended release micro-capsule, times of medicament taking is reduced, the potency of the medicament release is uniform, the safety is high, and a definite concentration of the medicament in the blood is sustained for a long time. The micro-capsule outer layer covers the original medicament, so that the rapid absorption of the medicament in the small intestine is ensured to rapidly achieve the concentration of the medicament in the blood for the treatment. The optimized structure of the pill can ensure that the medicament can be continuously and uniformly released while rapid onset of action is achieved, the concentration of the medicament in the blood can be sustained in a long time, and synthetic treatment effect and the feeling of the medicament taking by the patient is further enhanced.
EP2435571A2 Treatment of antiviral gene related diseases by inhibition of natural antisense transcript to an antiviral gene The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of an Antiviral gene, in particular, by targeting natural antisense polynucleotides of an Antiviral gene. The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of Antiviral genes.
EP2027081A2 Therapeutic prostaglandin compounds for the treatment of glaucoma Compounds having a structure are disclosed herein (Formula I). Compositions, methods, and medicaments related to the therapeutic use of these compounds are also disclosed.
CN1799542A Hawthorn fruit total flavone phospholipid composition and its preparation method The invention provides a hawthorn flavones and phosphatide compound and its preparation process, wherein the compound comprises phosphatide and hawthorn flavones by the molar ratio of 0.5-2 : 1, the preparing process consists of mixing phosphatide with hawthorn flavones, charging organic solvent with low dielectric constant, stirring, filtering, finally carrying out decompression drying or freeze drying.
CN102335125A Adrenaline hydrochloride injection and preparation process thereof The invention discloses an adrenaline hydrochloride injection and a preparation process thereof. The preparation process comprises the following steps: (1) adding water for injection in a container and inserting CO2 for 15 min, wherein, the volume of the water is 90% of the total volume, and the temperature of the water is less than 30 DEG C; (2) dissolving sodium chloride in proper amount of water for injection having a temperature of below 30 DEG C; (3) dissolving disodium edetate with boiled water for injection; (4) dissolving sodium chloride solution, disodium edetate solution, sodium pyrosulfite and epinephrine respectively in water for injection; (5) measuring the pH value of the solution, regulating the pH value to 3.6-4.0 with 1 mol/L hydrochloric acid, adding water for injection to reach the total amount, and uniformly stirring; (6) filtering; and (7) carrying out aseptic filling and sealing, and inserting N2 in ampoules when filling and sealing; or carrying out filling and sealing according to operating procedures of filling and sealing, inserting N2 in the ampoules when filling and sealing , and carrying out disinfection for 30 min at the temperature of 100 DEG C. The process realizes aseptic production, and products produced by the preparation process satisfy the national medicine quality standards.
CN1852894A Crystalline forms of [R-(r*,r*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid Novel crystalline forms of [R-(R*,R*)]-2-(4-fluorophenyl)-ss,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-l-heptanoic acid (atorvastatin free acid) designated Form A and Form B, characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease, and for preparing salts of atorvastatin.
CN102813640A Soft capsule containing desloratadine and preparation method thereof The invention belongs to the technical field of medicines and particularly relates to a soft capsule containing desloratadine and a preparation method thereof. Content of the soft capsule is prepared by esloratadine, antioxygen, dispersion media and suspending agents according to certain proportion, safety and stability of the soft capsule are improved by means of the soft capsule mode, so that the soft capsule is fast in dissolving, high in bioavailability, accurate in dose and fast in effect, the preparation method is simple, and the soft capsule is easy to produce and wide in application prospect.
CN103463018A Application of Lycojaponicumin B in preparation of medicine for treating hemorrhagic fever with renal syndrome The invention discloses a new application of Lycojaponicumin B in preparation of a medicine for treating hemorrhagic fever with renal syndrome. Experimental researches of the Lycojaponicumin B in-vitro and in-vivo inhibition on virus of hemorrhagic fever with renal syndrome indicate that the Lycojaponicumin B has low toxicity to cells, can directly kill the virus of hemorrhagic fever with renal syndrome, can remarkably inhibit multiplication of the virus, and can obviously protect shrewmouse infected by the virus so as to delay the disease time, prolong the course of disease and reduce the death rate. Therefore, the Lycojaponicumin B is an effective and safe medicine for treating hemorrhagic fever with renal syndrome.
WO2007083640A1 Preventive or remedy for increased urinary frequency and urinary incontinence [PROBLEMS] To provide a drug which has a selective β3 receptor activating effect and is useful in preventing or treating increased urinary frequency and urinary incontinence. [MEANS FOR SOLVING PROBLEMS] It is disclosed that 6-[2-(R)-[(2-[(R)-(3-chlorophenyl)-2-hydroxyethyl)amino]propyl]-2,3-dihydro-1,4-benzodioxy-2-(R)-carboxylic acid or a pharmacologically acceptable salt thereof is efficacious in preventing and treating increased urinary frequency and urinary incontinence, in particular, increased urinary frequency and urinary incontinence caused by hyperactive bladder.
DE102009057267A1 Ointment, useful for treating Mortellaro's disease in cloven-hoofed animals, comprises a mixture of cereal hydrolyzate, acid whey and water, where the mixture is added with calcium chloride, magnesium chloride and iron saccharate Ointment comprises a mixture of cereal hydrolyzate, acid whey and water, where the mixture is added with calcium chloride (900-3000 mg), magnesium chloride (500-190 mg) and iron saccharate (85-190 ml) each based on 100 g of the mixture. - ACTIVITY : Antiinflammatory; Dermatological. Test details are described but no results given. - MECHANISM OF ACTION : None given.
WO2008138350A1 Prevention of intraocular fibrosis The present invention relates to compounds capable of inhibiting intraocular fibrosis and their use for treatment and prevention of conditions that threaten visual function with specific emphasis on the prevention and treatment of subretinal fibrosis in eyes with subretinal choroidal neovascularization secondary to age-related macular degeneration, myopia, choroidal rupture, choroiditis, angioid streaks, and similar conditions, and the prevention and treatment of preretinal fibrosis secondary to neovascular proliferative retinopathy, retinal vein occlusion, sickle cell disease, uveitis, retinopathy of prematurity, proliferative vitreoretinopathy, traction retinal detachment, rubeosis iridis, neovascular glaucoma, and other diseases of the retinal and/or optic nerve characterized by the development of scar tissue within or adjacent to nervous tissue or elsewhere.
US8106065 Antitussive agent An antitussive, which can be used for therapy or prophylaxis of coughing, is disclosed. The antitussive comprises as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic substituent or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as the compound below [N-(17-cyclopeopylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-3,4,5,6-tetrahydrophthalimide]. The antitussive has an excellent therapeutic or prophylactic effect against coughing and the side effects thereof are small.
CN101199615A External for ¥ ²oral administration orally disintegrating tablets for treating recurrent oral ulcer and preparing method thereof The invention relates to an external and internal oral disintegrating tablet for treating dental ulcer and the preparation method, which comprises bee glue, indigo pulverata levis, peppermint, camphor, liquorice, borneol, borax, Chinese goldthread and plant soot having useful treatment quantity and medicine excipient that can rapidly release medicament by disintegration in the mouth. The disintegrating time in the mouth is within 40 seconds. Wherein, the medicine excipient includes bulking agent, disintegrating agent, corrigent, glidant, lubricant and effervescent. The invention is characterized in that the oral disintegrating tablet for curing dental ulcer has the integrated external and internal medicine taking function.
US20120093837 Compositions and methods for detecting egfr in cancer The invention discloses binding agents to the E746-A750 deletion and the L858R point mutations in the epidermal growth factor receptor (EGFR) molecule, and methods for use thereof, including methods for the diagnosis and treatment of cancer.
US20120202774 Acyloxy- and phosphoryloxy-butadiene-fe(co)3 complexes as enzyme-triggered co-releasing molecules The present invention provides acyloxy- and phosphoryloxy-butadiene-Fe(CO)3 complexes which can deliver carbon monoxide to a physiological target, wherein release of carbon monoxide can be enzymatically-triggered. The present invention also provides for methods of manufacturing the enzymatically-triggered carbon monoxide releasing molecules and methods for their use.
US20130035342 Compound Suitable for the Treatment of Synucleopathies The present invention relates to a compound of formula (I): Wherein R1 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; R2 is an alkyl group with 1 to 18 carbon atoms or a substituted or unsubstituted cycloalkyl or aryl group; R3 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; L is a single bond, an alkyl group having 1 to 6 carbon atoms, NHCO, O, S, NHCONH or NHCOO; X, Y and Z are independently 0, N, NH, S or CH; W is a single bond or an alkyl group having from 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate of said compound or salt.
US20090238757 Methods and Compositions for Administering Therapeutic and Diagnostic Agents Methods and compositions are described for targeting therapeutic and diagnostic molecules to particular types of cells using targeting antibodies or other targeting moeities.
CN102309455A Dexamethasone sodium phosphate powder injection and production method thereof The invention discloses a dexamethasone sodium phosphate powder injection and a production method thereof. The method for preparing the dexamethasone sodium phosphate powder injection comprises the following steps of: 1) dissolving dexamethasone sodium phosphate in an organic solvent to obtain a medicinal solution (1); and 2) performing sterilization and pyrogen removal on the medicinal solution (1), directly filling into an injection bottle, removing the organic solvent from the filled injection bottle by adopting a reduced-pressure drying method, capping and packaging, and recovering the organic solvent at the same time.
US20110229532 Process for nanoemulsification of curcumin and derivatives of curcumin A process for nanomulsification of highly lipophillic polyphenols compounds using non-ionic surfactant and a non-ionic co-solvent with the help of sonar energy, to enhance the aqueous solubility is disclosed herein.
WO2013032201A2 Material for preventing adhesion, and method for preventing adhesion The present invention relates to a material for preventing adhesion including hyaluronic acid, carboxymethyl cellulose, and alginate, and to a method for preventing adhesion at a local tracheal surface using the material for preventing adhesion. The material for preventing adhesion according to the present invention, which includes hyaluronic acid, carboxymethyl cellulose, and alginate, exhibits superior biocompatibility, in-vivo sustainability, and tissue cohesion properties, and thus can ultimately exhibit the effect of excellent adhesion prevention.
CN103565903A Cream for treating punctum The invention discloses a cream for treating punctum. The cream comprises the following components by weight according to the state of an illness of a general patient: 40-100g of egg white, 30-120g of castor fat juice, 10-20g of clay, 25-40g of pine nuts, 5-15g of copper chlorophyll and 10-20g of carbomer.
WO2014103862A1 Obesity preventive or therapeutic agent and rheumatism preventive or therapeutic agent [Problem] To provide a synoviolin-protein-ubiquitination-activity inhibitor, and a drug which is effective as an obesity preventive or therapeutic agent. [Solution] The present invention pertains to a synoviolin-protein-ubiquitination-activity inhibitor and an obesity preventive or therapeutic agent which contain a prescribed naphthalene derivative, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.
US8202845 Means and methods for the specific modulation of target genes in the CNS and the eye and methods for their identification Provided are methods for the treatment of disorders of the central nervous system (CNS) and the eye. In particular, use of compositions comprising a compound capable of modulating a target gene or gene product is described for the preparation of a pharmaceutical composition for the treatment of disorders of the CNS and/or the eye, wherein the composition is designed to be administered outside the blood-CNS and the blood-retina barriers. Furthermore, methods are provided for identifying and obtaining nucleic acid molecules encoding polypeptides involved in CNS disorders or of the eye, methods for diagnosing said disorders as well as transgenic animal deficient in the expression of target genes identified in accordance with the described method. In addition, methods of identifying and isolating drugs that are particularly useful for the treatment of disorders related to the CNS and/or the eye are disclosed.
WO2007031832A2 Use of bipyridine compound 'caerulomycin a' derivatives and analogs thereof as immunosuppressive agents The present invention relates to an isolated bioactive molecule Caerulomycin A, derivatives and analogs thereof as effective immunosuppressive agents. The immunosuppressive property of the compound is targeted in particular against the lymphocytes, CD4+ T cells, CD8+ T cells and B cells and in the production of IL-4 and IFN-Ϝ and antibodies. The compound operates through a mechanism by downregulating the expression of activation marker CD28 and upregulating the immunosuppressive marker CTLA-4. Caerulomycin A has previously been isolated from Streptomyces caeruleus and found to have useful antifungal activity. Prior to the present invention however, this compound had not been determined to have immunomodulatory activity.
CN102160685A Atomized caffeine and atomization method The invention discloses atomized caffeine and a generation method thereof. The invention is characterized in that: caffeine or a matter containing caffeine (such as tea, coffee or products, extracts thereof) is mixed with an unharmful combustible and prepared into tobacco or cigarettes; and during use, the ignited combustible and the caffeine can be atomized, the mist is inhaled and can refresh, and the burning mist of the combustible is unharmful; or caffeine or a matter containing caffeine is atomized by an atomization device (such as ultrasonic waves or/and propellants, compressed gases, heating elements and the like, or a stepwise atomization method).
US20090117076 Methods For Treating Tumor Cells Methods of treating a disease in a patient are disclosed that include the administration of a targeted therapy in combination with an immunotherapy. Such therapy is useful in the treatment of any disease susceptible to targeted therapy and attack by the immune system.
US20100210730 N-halogenated amino acid formulations with anti-inflammatory compounds The present invention relates to a formulation having antimicrobial activity comprising a N-halogenated amino acid and a anti-inflammatory compound. This specification also describes methods for treating a tissue infection comprising contacting the infected tissue with a pharmaceutically effective amount of a formulation comprising a N-halogenated amino acid and a anti-inflammatory compound. This specification further describes a method for treating respiratory infections comprising contacting the site of the respiratory infection with a pharmaceutically effective amount of a formulation comprising a N-halogenated amino acid and a anti-inflammatory compound.
US20110263645 Compositions and Methods of Treating Retinal Disease Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed
EP2515910A1 Use of polysaccharides for treating stress and anxiety The present invention relates to a composition including a mix of a polysaccharides having: 15% to 50% of glucoside linkages 1-6; a reducing sugar content of less than 20%; a polymolecularity index of less than 5; an average molecular weight with number Mn of less than 4500 g/mole and at least one active agent for treating stress, anxiety and depressive behaviour, sleep disorders, obsessive-compulsive disorder, bulimia and epilepsy in humans or animals. The present invention also relates to the use of said polysaccharide for treating stress, anxiety or depressive behaviour, sleep disorders, obsessive-compulsive disorder, bulimia and epilepsy in humans or animals.
US20120040003 Anti-dandruff compositions with citrus fibers A shampoo composition is described which includes from 1 to 25% by weight of mild surfactants, from 0.001 to 5% by weight of citrus fibers, from 0.01 to 5% by weight of anti-dandruff zinc salts, and a cosmetically acceptable carrier. The citrus fibers help structure the composition to maintain phase stability, provide appropriate viscosity and achieve deposition of the anti-dandruff zinc salts.
CN103330884A Ointment for treating dermatitis The invention relates to an ointment for treating dermatitis. The ointment is prepared by the following steps: preparing golden cypress, Agastache rugosus, pollen typhae, radix stemonae, Chinese lobelia, edible tulip, rhizoma atractylodis, rumex japonicus root, Jacaranda flower, radix angelicae and radix sophorae flavescentis; adding water which is 5-7 times mass of the medicinal materials, detecting for 2-3 hours; removing dregs; concentrating the medicine liquid to prepare a thick paste for later use; preparing snake oil and stearic acid; heating to 80-90 DEG C and maintaining the temperate so that snake oil and stearic acid are melted; additionally taking boiling water which is equal to stearic acid in mass, as well as triethanolamine, glycerol and sodium benzoate, heating to 80-90 DEG C and maintaining the temperate; gradually adding into the melted snake oil and stearic acid; continuously stirring; after uniformly stirring, cooling to emulsus; after temperature is reduced to below 30 DEG C, grinding borneol and alums to fine paste; and adding the thick paste for later use and uniformly stirring. The ointment provided by the invention effectively treats dermatitis, eczema and the like, and is convenient to use, and meanwhile, lesion and drug dependence possibly caused by Western medicines can be avoided.
US20080075758 Non-Antibiotic Intervention of Chlamydial Infection Methods for treating or reducing the risk of transmission of chlamydia to a recipient by topically applying a metalloprotease inhibitor to a site on the recipient which is likely to be exposed to Chlamydia. Topical compositions containing metalloprotease inhibitors are also disclosed for treating or reducing the risk of transmission of Chlamydia, as well as barrier contraceptive devices coated therewith.
US20110280893 Synthetic lipid a derivative The invention provides functionalized monosaccharides and disaccharides suitable for use in synthesizing a lipid A derivative, as well as methods for synthesizing and using a synthetic lipid A derivative.
CN101591347A Cefixime acid type double salt compound and preparation method thereof The invention provides an acid type double salt with a chemical name of (6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-(carboxymethoxyimino)acetamido]-3-ethylene-8-oxo-5-thia-1-azabicyclo[4,2,0]-octo-2-ene-2-carboxylic acid. A preparation method comprises the following steps: reacting cefixime with sulfuric acid or phosphoric acid to prepare a cefixime acid salt; reacting the cefixime acid salt with MOR in a polar solvent, and concentrating the reaction product; crystallizing the reaction product with a weak polar solvent; and filtering the reaction product, and drying the solid to obtain the cefixime acid type double salt. The preparation method has the advantages of reasonable design, simple process and low cost. The cefixime acid type double salt prepared by the method has the characteristics of high purity and content, good stability, difficult generation of polymers and the like. Medicaments prepared from the cefixime acid type double salt can overcome the defects that cephalosporins are easy to generate the polymers, can cause strong anaphylactic reactions and the like.
CN102580094A Medicine for treating fowl plague and duck plague The invention belongs to the technical field of veterinary medicines, and provides a medicine for treating fowl plague and duck plague. The medicine is characterized by being prepared from the following raw material medicines: 10-30 parts of antiphologistic powder, 20-40 parts of neomycin and 10-30 parts of synergist. Tests prove that the medicine can effectively treat fowl plague and duck plague, and has the advantages of being high in curative effect, time-saving and labor-saving.
CN101683342A Methylphenidatefrozen dry powder preparation for injection and preparation process thereof The invention relates to a methylphenidatefrozen dry powder preparation for injection and a preparation process thereof; the preparation takes the salt of the methylphenidatefrozen as drug constituents and forms the drug composite by mixing acceptable accessories pharmaceutically; the preparation method is that: the salt of the methylphenidatefrozen is taken as raw material, the accessories with specific kinds and proportion are added, and the dry powder preparation for intravenous injection is prepared and developed by adopting the illustrative technological measures. The dry powder preparation is used for treating attention deficiency hyperkinetic disorder (hyperkinetic syndrome of children and mild brain functional maladjustment), and eliminating somnolence, lassitude and respiratory depression caused by soporifics.
US20080166398 Antifungal Compositions Pharmaceutical compositions useful for treating dermal diseases caused by fungi and yeasts with inflammation and/or associated with a bacterial infection. Such compositions contain a therapeutically effective amount of sertaconazole, or a pharmaceutically acceptable salt, solvate, isomer thereof or mixtures thereof; and a therapeutically effective amount of at least one compound selected from the group consisting of hydrocortisone, a pharmaceutically acceptable ester of hydrocortisone, an antibacterial quinolone compound, and mixtures thereof.
US20090169504 Compounds and Pharmaceutical compositions for the treatment of Viral infections Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
CA2266342C Packaging cell lines for use in facilitating the development of high-capacity adenoviral vectors The present invention relates to gene therapy, especially to adenovirus-based gene therapy, and related cell lines and compositions. In particular, novel packaging cell lines are disclosed, for use in facilitating the development of high-capacity vectors. The invention also discloses a variety of high-capacity adenovirus vectors and related compositions and kits including the disclosed cell lines and vectors. Finally, the invention discloses methods of preparing and using the disclosed vectors, cell lines and kits.
WO2014101115A1 Montelukast sodium tablet composition and preparation method thereof A Montelukast Sodium tablet composition and a preparation method thereof. The composition comprises Montelukast Sodium, a porous filling agent, a disintegrating agent, a lubricant, an opadry film coating premixing agent, and purified water. A method for preparing the porous filling agent comprises: dissolving a filling agent and then spray-drying the filling agent; or dissolving a filling agent, adding and uniformly dispersing a disintegrating agent in the filling agent, and then spray-drying the filling agent. The preparation method of the Montelukast Sodium tablet composition adopts a direct powder compression method.
US7326708 Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor The dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The invention also relates to a crystalline monohydrate of the dihydrogenphosphate salt as well as a process for its preparation, pharmaceutical compositions containing this novel form and methods of use for the treatment of diabetes, obesity, and high blood pressure.
US7790725 Thiazolidine derivatives and medicinal use thereof A thiazolidine derivative represented by the formula (I) wherein each symbol is as defined in the specification, and a pharmaceutically acceptable salt thereof exhibit a potent DPP-IV inhibitory activity, and can be provided as an agent for the prophylaxis or treatment of diabetes, an agent for the prophylaxis or treatment of obesity and the like.
US20060258726 1,5-Disubstituted imidazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of eye and bone diseases This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors of formula (I), their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of the patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
EP1627635A2 Benzothiazolium compounds for use in methods of inhibiting NO production and TNF alpha and treating coronaviral infection This invention relates to a method of inhibiting NO production and TNFα and treating coronaviral infection by administering an effective amount of a compound of the following formula: wherein R1, R2, R3, R4, R5, A, and X are as defined herein.
WO2012002922A1 Synergistic pharmaceutical formulations of colesevelam and fenofibrate The present invention relates to a new synergistic combination of active agents belonging to bile acid binding group and pharmaceutical compositions comprising said combination.
US20110160186 Methods of Treating CYP2D6 Alternative Metabolizers The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.
US20100056521 (aza)indole derivative and use thereof for medical purposes The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, nitro, alkyl, alkoxy and the like; X1, X2 and X3 independently represent CR2 or N; R1 and R2 independently represent halogen, cyano, haloalkyl, A-D-E-G, —N(-D-E-G)2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO2 and the like.
CN102670557A Lovastatin osmotic pump controlled release tablet The invention provides a novel lovastatin osmotic pump controlled release tablet. Ethyl cellulose and polyvidone are taken as semi-permeable membrane forming materials, and asymmetrical tablets are provided preferably, so that the phenomenon of ageing of a semi-permeable membrane can be avoided, and medicament residues are reduced. The invention further provides a method for improving the anti-ageing performance of the lovastatin osmotic pump controlled release tablet. The method is characterized in that: ethyl cellulose-polyvidone is taken as a semi-permeable membrane material. Moreover, the invention further provides an application of an ethyl cellulose-polyvidone composition to preparation of a lovastatin osmotic pump controlled release tablet with anti-ageing performance.
CN1631371A Oral administered bitter free powder of macrolide antibiotic, its prescription and preparation process The invention relates to an oral administered bitter free powder of macrolide antibiotic, its prescription and preparation process, wherein the powder prescription comprises macrolides antibiotics, lubrication flow auxiliary agent, high molecular polymer, sweetener and flavoring agent. The prescription has good taste, high dissolution and biological availability, thus is suitable of the administration by adults, children, the elderly and patients of dysphagia. The dosage types can be expanded to granule, dried mixing suspension agent and dispersion tablet.
EP0931060B1 Substituted n- (aminoiminomethyl or aminomethyl)phenyl propyl amides This invention relates to compounds of formula (I) which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
US7227014 Oligonucleotide with 8-50 bases specifically hybridizes with a nucleic acid molecule encoding human apolipoprotein(a) and inhibits its expression Antisense compounds, compositions and methods are provided for modulating the expression of apolipoprotein(a). The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding apolipoprotein(a). Methods of using these compounds for modulation of apolipoprotein(a) expression and for treatment of diseases associated with expression of apolipoprotein(a) are provided.
US20110178163 Mir-182 in the diagnosis and treatment of cancer The present disclosure provides methods of determining the levels of BRCA1 in a cell, altering the levels of BRCA1 in a cell, determining the likelihood of developing cancer, and determining the prognosis of a patient with cancer using miR-182 and analogs thereof. Importantly, the invention also provides methods of determining whether a patient should be treated with PARP inhibitors, improving PARP therapy in cancer, as well as methods for selecting and improving genotoxic therapies. Also featured are methods of treating patients with cancers based on the expression levels of miR-182. The invention also features compositions comprising miR-182 and analogs thereof, antagomirs of mIR-182 and analogs thereof, in combination with PARP inhibitors and genotoxic agents.
US20110306635 Pyridine compounds as subtype selective modulators of alpha2b and /or alpha 2c adrenergic receptors The invention relates specifically to the use of certain 4-[1-(1H-Imidazol-4-yl)-ethyl]-2,3-substituted pyridine compounds and pharmaceutical compositions thereof to treat disorders associated with selective subtype alpha 2 adrenergic receptor modulation.
US20120122837 Inhibitors of fatty acid binding protein The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
WO2013173436A1 Pre-selection of subjects for therapeutic treatment with an hsp90 inhibitor based on hypoxic status The present invention provides methods for the pre-selection of a subject for therapeutic treatment with an Hsp90 inhibitor based on modulated levels of hypoxia in cancerous cells in the subject. In one embodiment, the invention provides methods for the pre-selection of a subject for therapeutic treatment with an Hsp90 inhibitor based on modulated levels of lactate dehydrogenase (LDH) in a cell, e.g., a cancerous cell. The invention also provides methods for treating cancer in a subject by administering an effective amount of an Hsp90 inhibitor to the subject, wherein the subject has been selected based on a modulated level of hypoxia. The invention further provides kits to practice the methods of the invention.
WO2006131398A3 Inhibitors of soluble adenylate cyclase The invention relates to compounds of general Formula (I), the production thereof, and the use thereof as a medicinal product.
WO2008151437A1 Heme-oxygenase inhibitors and use of the same in the treatment of cancer and diseases of the central nervous system Disclosed are compounds of the general formula (1): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.
US20100216706 Ghrelin Protects Substantia Nigra Dopamine Neurons A method of treating neurodegeneration of substantia nigra pars compacta (SNpc) dopamine neurons and compositions therefor are provided.
WO2006064754A1 Preventive or therapeutic agent for sleep disorder A combination of (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide with a medicine capable of prolonging a slow-wave sleep time provides a preventive or therapeutic agent for sleep disorder that induces natural sleep, shortens sleep latency, increases deep sleep, excels in sleep sustention and ensures an appropriate sleep time.
EP1268305B1 Infusion packet with useful and decorative elements, support member, delivery system and method A system allowing the tea bag/infusion packet (14) to dispense health enhancing agents and promote the sale and use of safe and health enhancing beverages. The basic packet (14) is a permeable sac containing soluble ingredients tethered to a tag (16). In one embodiment soluble dietary fiber, nutraceuticals, enzymes, and other health promoting ingredients are dispensed. In one embodiment the tag (16) forms part of a game, acts as a prize, or toy, or otherwise promotes the sale and use of the product. In one embodiment the packet (14) is modified to change color or reveal indicia upon contact with water. An additional support member may be supplied to hold or join the infusion packets (14) and may act as a toy, or prize, or game piece. For use in bottles, such as water bottles, a version is provided with features to prevent accidental ingestion of the infusion packet (14).
CN103739471A Beta-hinokitol derivative and application thereof in preparation of special antibacterial agent for animals and antimicrobial growth promoter for feed The invention discloses a beta-hinokitol derivative and application thereof in preparation of a special antibacterial agent for animals and an antimicrobial growth promoter for a feed. A structural formula of the beta-hinokitol derivative is shown as a formula (I), wherein R is n-propyl, n-amyl group, benzyl group, sec-butyl, ethyl, normal-butyl, 4-chlorobenzyl), 4-fluorobenzyl, n-octyl, 1-fluoropropyl or n-tetradecanamide. The beta-hinokitol derivative shown as the formula (I), provided by the invention, has low toxicity or non-toxicity to beasts and birds, higher safety and stronger growth promoting performance in comparison those of relevant compounds covered by an existing patent, thereby being more suitable for being used as a growth promoter for the feed, and being very good in application prospect in the cultivation industry. The formula (I) is described in the description.
US20080096963 Especially bee stings; linoleic acid, oleic acid, lauric acid, myristic acid, palmitic acid, stearic acid, arachidic acid, behenic acid, lignoceric acid, or palmitoleic acid; also administered by injection; ointments, creams, gels, patches, powders, sprays, lotions, sticks; antiallergens, antihistamines The invention relates to the use of a fatty acid for preparing a composition for allaying inflammatory reactions due to hypenoptera stings.
US20080207735 1-Amino Linked Compounds The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
WO2014047111A1 Sgc stimulators Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
CN101492440B Separation purification process for main catechin component in tea polyphenol and glycosidase activity The invention discloses a separation and purification method of main catechin components in tea polyphenol and glycosidase activity thereof. In the separation and purification method, tea polyphenol extracts are absorbed by macroporous adsorption resin of nonpolar or weak polar polystyrene; water and ethanol are used for the elution; alcohol eluates, through polyamide columns for the chromatography and are eluted respectively by water and ethanol. The water recrystallization is carried out on the alcohol eluates of the polyamide columns to obtain EGCG pure products with the purity larger than95 percent and the yield larger than 50 percent; reversed-phase C18 filled columns are used for the chromatography of water eluates of the polyamide columns to obtain EC and EGC; the ethanol of 50-80percent is used for the recrystallization to obtain pure products of the EC and EGC with the purity all larger than 96 percent. Tests in vitro show that EGCG, EGC and EC all have inhibitory activity on alpha-glucosidase and alpha-amylase and can be used for preparing weight reduction products reducing the absorption of carbohydrates or drugs or health products lowering the postprandial blood glucose.
CN102652758A Application of health care drinking liquid containing deep seawater in preparation of medicaments or health care products for preventing or treating hyperlipidemia The invention provides an application of health care drinking liquid containing deep seawater in the preparation of medicaments or health care products for preventing or treating hyperlipoidemia. The health care drinking liquid comprises A liquid and B liquid, wherein the A liquid is of fresh water, the B liquid is of high-concentration concentrated liquid which is obtained by performing decompression concentration on a concentrated water part which is separated from the deep sweater via a reverse osmosis device, and the hardness range is 200-1000ppm. The health care drinking liquid is given to a rat with the hyperlipoidemia, which is subjected to modeling by a high-fat emulsion, in a free drinking way, after the medicament is administrated for 28 days, the blood lipid level of the rat with the hyperlipoidemia can be significantly reduced, lipid peroxidation can be inhibited, the activity of lipoprotein metabolic enzymes, namely LCAT (lecithin-cholesterol acetyltransferase), LPL (lipoprotein lipase) and HL (hepatic lipase), can be significantly improved, and the state of lipid metabolism disorder in the rat with the hyperlipoidemia, as well as concurrent fatty liver and diabetes thereof, can be further improved. The health care drinking liquid is derived from the deep seawater, has the advantages of abundant resources, easiness in industrialization and the like, and further has broad market and application prospects in the aspect of preventing and treating the hyperlipoidemia.
CA2390472C Anti-inflammatory actions of cytochrome p450 epoxygenase-derived eicosanoids Epoxyeicosatrienoic acids (EETs) are products of cytochrome P450 epoxygenases that have vasodilatory properties similar to endothelium-derived hyperpolarizing factor (EDHF). The cytochrome P450 isoform CYP2J2 was cloned and identified as a source of EETs in human endothelial cells. Physiological concentrations of EETs or overexpression of CYP2J2 decreased cytolcine-induced endothelial cell adhesion molecule expression and prevented subsequent leukocyte adhesion to the vascular wall by a mechanism involving inhibition of transcription factor NF-.kappa.B and I.kappa.B kinase (IKK). The inhibitory effects of EETs were independent of their membrane hypopolarizing effects suggesting that these molecules play an important non-vasodilatory role in vascular inflammation.
US20120149751 Antiviral Drugs for Treatment of Arenavirus Infection Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
US20110071124 Compounds that Inhibit Production of sAPPB and AB and Uses Thereof The present invention relates to compounds with activity as inhibitors of sAPPβ and Aβ production, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease and pharmaceutical compositions containing such candidate compounds.
US20090186896 PDE Inhibitors and Combinations Thereof for the Treatment of Urological Disorders The invention provides pharmacological compositions comprising PDE-5 and PDE-4 inhibitors, alone or in combination, for the treatment of urological disorders comprising Benign Prostate Hyperplasia (BPH), Lower Urinary Tract Symptoms (LUTS) and in particular irritative symptoms caused by BPH-induced bladder outlet obstruction (BOO). The invention also provides methods of screening for such PDE-5 and PDE-4 inhibitors for use, alone and in combination, in the preparation of medicaments for the treatment of said urological disorders.
EP1381392A4 Synthetic catalyst for selective cleavage of protein and method for selective cleavage of protein using the same The present invention relates to a synthetic catalyst which can selectively recognize and cleave a specific protein among a protein mixture, and to a method for selective cleavage of a target protein using the same.
WO2007100027A1 Optically active thiazolidinedione derivative Disclosed are an optically active thiazolidinedione derivative, a pharmacologically acceptable salt thereof, and a pharmaceutical product containing any of them. The optically active thiazolidinedione derivative can be obtained by optical resolution of (RS)-5-{4-[(6-methoxy- 1-methyl-1H-benzoimidazol-2-yl)methoxy]benzyl}-1,3- thiazolidine-2,4-dione.
CN101091723A External remedy for curing purulent otitis media and preparation method The present invention relates to a medicine for external application for curing otitis media suppurativa and its preparation method. Said medicine prescription includes 5-6g of alum, 2-3g of borneol and 3-4g of fresh pig's bile. Said invention also provides the concrete steps of its preparation method.
WO2008030579A3 Irak modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder The present invention relates to modulators of IRAK kinase and provides compositions comprising such modulators, as well as methods therewith for treating conditions or diseases mediated by or associated with IRAK kinase, such as rheumatoid arthitis, multiple sclerosis, sepsis, osteoarthrites, inflammatory bowel disease, osteoporosis, myasthenia gravis, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, psoriasis, cardiac contractile dysfunction, type I diabetes, type II diabetes, familial cold autoinf lammatory syndrome, severe bacterial infections, allergic disease, cancer, psoriasis, asthma, or graft rejection.
CA2396702C N,o-amidomalonate platinum complexes The present invention relates purified platinum complexes in which platinum is coordinated to form a single N,O- or O,O-chelate of an amidomalonate. The chelates, and pharmaceutically acceptable formulations thereof, are useful for the treatment of cancer. The platinum chelates may additionally be linked to one or more functional groups which increases water solubility and/or assists in tumor targeting of the chelate. Examples of tumor targeting moieties include polymers, in which one or more platinum chelates are attached to the polymer backbone via linkers capable of being cleaved in the body, and molecules with a high affinity for receptors which are concentrated or upregulated in tumor tissue and/or the tumor vasculature.
WO2009030257A1 Methods and compounds for treating diseases caused by reactive oxygen species Provided is a method of treating a patient having an inflammatory disease by using a compound which inhibits the complex l-mediated ROS production, a medicament containing such compound and methods for screening for such compounds.
CN1969821A Anticancer medicament and synergist simultaneously carrying anticancer sustained release agent Disclosed is an anti-cancer slow release agent in the form of slow release injection or slow release implantation agent carrying both anti-cancer drugs and synergistic agent, the slow release injection comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The suspending agent is selected from carboxymethylcellulose, the viscosity of the suspension adjuvant is 80-3000cp (at room temperature). The anticancer active constituent being the combination of alkylating agent such as Melphalan and isoendoxan, purine analogues such as 06-BG and/or hormone group anti-cancer drugs selected from Triptorelin, Goserelin Leuprorelin and Epothilone and its derivatives (Epothilone A-F), the slow release auxiliary materials are selected from polylactic acid and its copolymer, Polifeprosan, polylactic acid copolymer or mixture, sebacylic acid copolymer or mixture. The slow release injection and slow release implanting agent can be used independently for effectively suppressing tumor accretion, or used in combination with non-operative methods such as chemotherapy and/or radiotheraphy with the function of improving their treatment effects.
US20100298395 Unsubstituted and substituted 4-benzyl-1,3-dihydro-imidazole-2-thiones acting as specific or selective alpha2 adrenergic agonists and methods for using the same Compounds of Formula 1 where the variables have the meaning defined in the specification are used to activate alpha2 adrenergic receptors. The compounds of Formula 1 are incorporated in pharmaceutical compositions and are used as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors.
US7452877 Irritable bowel disorders; controlling permeability of intestine tissue ; anticholinergic agent Methods are disclosed for treating hyperalgesia associated with irritable bowel syndrome comprising administering a direct and selective inhibitor of MLCK.
EP2628483A1 Medical adsorbent and method for producing same A medical adsorbent for oral administration that has low dosage and excellent adsorptive capacity and selective adsorption for toxins to be removed, and is also economical and environmentally friendly. The medical adsorbent comprises granular activated carbon that is activated carbon obtained by carbonization and activation of refined cellulose or regenerated cellulose, and having a mean pore diameter of 1.5 to 2.2 nm, a BET specific surface area of 700 to 3000 m2/g, a mean particle size of 100 to 1100 µm, a surface oxide content of 0.05 meq/g or greater and a packing density of 0.4 to 0.8 g/mL, and it can be used as a therapeutic or prophylactic agent for kidney disease or liver disease, for oral administration.
US20090111848 Halogenated Pyrazolo[1,5-A]Pyrimidines, Processes, Uses, Compositions and Intermediates The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.
WO2008123602A1 Therapeutic agent for arthropathy for intraarticular administration Disclosed are a therapeutic agent for arthropathy and a joint protective agent, both of which are intended to be administered intraarticularly. Specifically disclosed is a therapeutic agent for arthropathy for intraarticular administration, which comprises statin, a pharmaceutically acceptable salt thereof, or a solvate of statin or the salt as an active ingredient.
US20120059021 Compositions and methods for treating cancer and methods for predicting a response to such treatments The present disclosure relates to the regulation and function of the Wnt/β-catenin signaling pathway and the ERK signaling pathway. The disclosure provides methods of treatment for melanoma by administering both an inhibitor of ERK signaling and an activator of Wnt/β-catenin signaling. These methods may be used alone or in combination with other strategies targeting melanoma cell survival. The disclosure also provides diagnostic methods for predicting a patient's clinical response to inhibitors of ERK signaling.
CN103202847A Foreskin phimosis debonding liquid preparation method The invention relates to a foreskin phimosis debonding liquid preparation method. The method comprises the following steps: taking 20ml of a lidocaine hydrochloride gel, taking 1-6ml of a dexamethasone sodium phosphate injection, and fully mixing the gel and the injection. Foreskins are loosed, aches are mitigated and foreskin phimosis glans adhesion is easily solved several minutes after the medicinal liquid prepared through the method is sprayed on a male genitals. The medicinal liquid prepared through the method has anti-inflammation and anti-allergy effects.
US20110160187 3-aryl-5,6-disubstituted pyridazines The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.
CN102552202A Method for preparing xanthan gum omeprazole intragastric retention floating sustained-release tablets The invention relates to the field of medicinal preparations, in particular to a method for preparing xanthan gum omeprazole intragastric retention floating sustained-release tablets. Omeprazole is a new anti-peptic ulcer medicine which is studied and developed in recent years and of which the action mechanism is different from the antagonistic action of H2 receptors, but the half-life period of the medicine is 0.5 to 1 hour, so the effective medicinal concentration is necessarily improved by a new technology to improve the bioavailability of the medicine. According to the method, xanthan gum is used as a skeleton, additives such as a foaming agent are added to improve floating force, and CO2 released when the additives contact gastric acid is wrapped in a gel layer, so that the density of a preparation is easy to reduce or low-density hydrophobic substances are added to reduce the density of the preparation and prevent the hydration of the skeleton. Water-soluble medicines are prepared into hydrophilic gel skeleton tablets to solve the problem of controlling release speed, the skeleton releases the medicines by a dissolution mechanism, and the medicine release characteristic of an optimizing formula accords with a Higuichi equation, so that the bioavailability of the medicines is improved, and the action time is prolonged.
WO2012017434A3 Guanine nucleotide derivatives for treating bacterial infections The present invention generally relates to Rel proteins as a novel therapeutic target for treating bacterial threats. More specifically, the present invention relates to a novel class of compounds of formula (I) which inhibit RelA and/or Relseq and/or Rel/Spo synthetic activity or bacterial spore formation and which possess anti -bacterial activity. The present invention also relates to pharmaceutical compositions comprising such compounds, and to methods of use thereof for combating bacteria and treating bacterial infections.
CN101239936B Antineoplastic sulfur-containing alkannin and naphthoquinones derivatives The invention relates to an antineoplastic derivative of the medical technology field, which contains sulfur alkannin and naphthaquinone, i. e., 6-substituted 5, 8-dimethoxy-1, 4-naphthaquinone derivative and 2-substituted 5, 8-dimethoxy-1, 4-naphthaquinone derivative having a structure formula, wherein, R1 is 3-methyl-2-butenyl, methyl, n-propyl, n-pentyl; R2 is alkanoylindoles, aroyl and alkyl. The formula I is 6-substituted 5, 8-dimethoxy-1, 4-naphthaquinone and the formula II is 2-substituted 5, 8-dimethoxy-1, 4-naphthaquinone.
WO2013186857A1 Aptamer to fgf2 and use thereof Provided are: an aptamer which has an inhibitory activity on FGF2; a complex which comprises an aptamer that has a binding activity to or an inhibitory activity on FGF2 and a functional substance (for example, an affinity substance, a labeling substance, an enzyme, a drug delivery medium, a drug or the like); a pharmaceutical agent, a diagnostic agent and a labeling agent, each of which contains an aptamer that has a binding activity to or an inhibitory activity on FGF2, or a complex that comprises the aptamer and a functional substance; and the like.
WO2008089557A1 Atorvastatin calcium propylene glycol solvates The present application relates to atorvastatin calcium propylene glycol solvates and processes of preparing the same. The atorvastatin calcium propylene glycol solvates are crystalline and show high chemical and solid state stability, low hygroscopicity, and good flow properties.The solvates can be efficiently prepared from various forms of atorvastatin and either (R), (S), or mixtures of (R) and (S) propylene glycol, and may be easily filtered and dried on an industrial scale.
US6924292 Nitrogen compounds such as 2-(methylsulfinyl) N [3-(3,4,8,9-tetrahydro-6-methoxy-3,3,8,8-tetramethylfuro[2,3-h]isoquinolin-1-yl)phenyl]acetamide, used as phosphodiesterase inhibitors; antidiabetics; antiinflammatory agents A compound having a partial structure represented by Formula: or a salt thereof has an excellent phosphodiesterase (PDE) IV-inhibiting effect, and is useful as a prophylactic or therapeutic agent against inflammatory diseases, for example, bronchial asthma, chronic obstructive pulmonary disease (COPD), rheumatoid arthritis, autoimmune disease, diabetes and the like.
CN103445162A Pyruvoyl lauroyl glyceride and preparation method thereof The invention relates to pyruvoyl lauroyl glyceride and a preparation method thereof. According to the preparation method disclosed by the invention, pyruvoyl lauroyl glyceride is synthesized by direct esterification of pyruvic acid and lauric acid monoglyceride, wherein reduced-pressure distillation is adopted to remove water in the reaction, and the vacuum degree of a reaction system is 1KPa-30KPa. Pyruvoyl lauroyl glyceride prepared by the preparation method disclosed by the invention can partially replace grease to be used for salad oil and can be used as a nutrition intensifier; simultaneously, pyruvoyl lauroyl glyceride is a fat-soluble pyruvic acid series derivative and further becomes a functional food with great potential.
WO2006081280A1 3-heterocyclyl-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic and/or immunostimulant activity The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals.
WO2010055081A1 Use of leukotriene inhibitors for treating lung diseases in prematurely born infants The invention relates to the use of at least one leukotriene inhibitor for preparing a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants. The invention further relates to a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants, the pharmaceutical composition comprising at least one leukotriene inhibitor. The invention additionally relates to a method for the treatment and/or prophylaxis of a lung disease, more particularly of a bronchopulmonary dysplasia, in a prematurely born infant, where the prematurely born infant is administered a pharmacologically active amount of at least one leukotriene inhibitor.
EP1845954A2 Orally disintegrating composition of olanzapine or donepezil The invention relates to orally disintegrating compositions of olanzapine or donepezil which show a very quick release of the active ingredient, as well as a process for their preparation.
CN103610079A Application method of DHA (Dihexyl Adipate) phospholipid The invention provides novel use of DHA (Dihexyl Adipate) phospholipid, i.e., application of DHA phospholipid in preparing a sleep-aiding product. A preparation method of the DHA phospholipid disclosed by the invention comprises the following steps: firstly, extracting materials by extracting liquor, collecting lower-layer liquor after stewing and layering; removing water by using anhydrous sodium sulfate, drying by distillation to obtain total lipid, thus obtaining a crude product after adding cold acetone to wash, and the like; and purifying the crude product to obtain the DHA phospholipid. The DHA phospholipid disclosed by the invention is pure natural extract, high in safety, good in stability, and easier to absorb by a human body, and has a very high nutritional value and healthcare function. Applying effect of mice indicates that sleep time of the mice can be effectively promoted. And therefore, the DHA phospholipid has application potential of being developed into the sleep-aiding product.
WO2007053094A1 CHROMAN COMPOUNDS AS 5 -HTlB ANTAGONISTS Chroman derivatives according to Formula (I) below: wherein R1, R2, R3 ,and R4 are as defined in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical .compositions containing and methods for using the'' same. The compounds are 5-HT1B antagonists and are useful in the treatment of mood and . anxiety disorders as well as cognitive disorders.
US20100249123 Novel benzamide derivatives as modulators of the follicle stimulating hormone The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1 n are defined as in formula I; invention compounds are modulators of follicle-stimulating hormone—(“FSH”) which are useful for male and female contraception as well as other disorders modulated by FSH receptor.
EP1558599A2 Heteroarylpiperidine modulators of chemokine receptor activity The present invention is directed to compounds of the formula (I): (wherein R1, R2, R3, R4, R5, R6, R10 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
CN101880265A Acid-sensitive polymeric micelle pharmaceutical composition and preparation method thereof The invention relates to a synthesis method of an amphiphilic block polymer of which the side chain contains acid-sensitive matrixes (ortho-esters), a delivery carrier thereof and a pH-sensitive controlled-release micelle pharmaceutical composition containing an activator. The pharmaceutical composition can be a partial controllable delivery preparation formulation or an injectable preparation formulation for the activator. Hydrophobic medicines can be loaded in the micelle easily by using a simple method, and the polymeric pharmaceutical composition can greatly improve the intracellular transmission efficiency of medicines and the killing efficiency of cancer cells.
WO2007070067A1 Regeneration of vaginal tissue with non-systemic vaginal administration of estrogen Methods and formulations for the regeneration of vaginal tissue and vaginal cell health resulting from vaginal cell hypoxia in a human female. A pharmaceutical composition for topical non-systemic administration is formulated containing a hormonal agent administered to the vagina, vulvar area of the individual undergoing treatment.
WO2009148163A1 Agent for contracting bladder detrusor muscle and relaxing urethral sphincter muscle Provided is a highly safe and excellent preventive, remedy and/or symptom-relieving agent for underactive bladder which has both of an effect of promoting the contraction of the bladder detrusor muscle and an effect of relaxing the urethral sphincter muscle and shows a strong urination effect. Because of having an effect of promoting the contraction of the bladder detrusor muscle and an effect of relaxing the urethral sphincter muscle and thus being capable of relieving bladder contraction disorders and urethral relaxation failures, a compound represented by general formula (I) is efficacious as a preventive and/or remedy for underactive bladder. Moreover, the compound represented by general formula (I) never induces side effects, for example, bladder irritation exerted by PGE1, PGE2 or EP1 agonist or EP3 agonist. Thus, the compound represented by general formula (I), a salt thereof, an N-oxide thereof, an S-oxide thereof and a solvate thereof or prodrugs or cyclodextrin clathrate compounds of the same are useful as a highly safe and excellent preventive, remedy and/or symptom-relieving agent for underactive bladder.
US20120171123 Uses and compositions for treatment of rheumatoid arthritis The invention provides methods, uses and compositions for the treatment of rheumatoid arthritis. The invention describes methods and uses for treating rheumatoid arthritis wherein a TNFα inhibitor, such as a human TNFα antibody, or antigen-binding portion thereof. Also described are methods for determining the efficacy of a TNFα inhibitor for treatment of rheumatoid arthritis in a subject.
CN101697967A Adapalene-vitamin E compound cream and preparation method thereof The invention relates to compound cream containing adapalene and vitamin E and a preparation method thereof. The preparation contains 0.08 to 0.20 weight percent of adapalene and 0.08 to 0.12 percent of vitamin E. The preparation method of the adapalene-vitamin E compound cream comprises: preparing an oil phase and a water phase; preparing medicament solution; and pouring the oil phase into the water phase for emulsification, adding the medicament solution after cooling, and fully stirring for even mixing. The prepared oil-in-water compound cream, which is uniform, delicate, easy to coat and clean, high compatible with skin and high stable, can be used for treating chloasma and has a health-care and nourishing effect on skin.
EP1586644A2 Medicament for the prevention and/or the treatment of ischemic heart and peripheral vascular diseases, tumour development and for wound healing The present invention is related to a compound or a pharmaceutical composition thereof for the use of a medicament in the modulation of angiogenesis through the tackling of the intracellular free cholesterol-caveolin1-eNOS-NO pathway. The present invention also provides a method of study, testing, screening and manufacturing of new compounds or compositions which influences the angiogenesis via said pathway with the aim of identifying a compound or composition having possible therapeutic or prophylactic properties upon ischemic heart and peripheral vascular diseases including cerebral diseases, tumour development and wound healing.
CN101332293A High-calcium soft chewable tablets and production method The invention provides a high-calcium soft chewable tablet and a manufacturing method thereof, which belongs to the field of health care food. The high-calcium soft chewable tablet is made of raw materials with the weight proportion by parts: 5 to 30 parts of edible calcium, 0.2 to 0.5 part of kelp extract, 0.005 to 0.01 part of casein phospho peptides, 20 to 60 parts of edible sugar, 5 to 15 parts of mineral water or purified water, 0.05 to 0.3 part of vitamin, 0.5 to 3 parts of edible gelatine and 0.1 to 0.5 part of food additive. The invention has the manufacturing method that the edible sugar, the mineral water or purified water, the edible gelatine, the edible calcium are evenly mixed according to the weight proportion by parts and put into a sugar cooker for boiling into a pasty form, then the kelp extract, the vitamin, the casein phospho peptides and the food additive are added, and then cooling, drying and packing are carried out after the mixed materials are formed into a soft tablet by a perfusion unit. Compared with the prior art, the high-calcium soft chewable tablet of the invention has the advantages of low manufacturing cost, good taste, fast absorption, wide applicable range of people, obvious calcium-enriching effect and on the like, thereby largely breaking through the difficulties of the taste and the absorption of the hard calcium tablet in the prior art. The manufacturing method has simple technology and less device investment.
CN103356519A Application of dihydromyricetin in induction of cancer cell autophagy The invention discloses an application of dihydromyricetin in preparation of an autophagy inducer for inducing cancer cell autophagy. The experiments prove that the dihydromyricetin can effectively induce cancer cell autophagy. Meanwhile, the experiments prove that the dihydromyricetin is expressed by multi-level inhibition of a main protein mTOR in an intracellular autophagy inhibition pathway in two aspects of reducing the ErK protein expression and improving the AMPK protein expression, and the intracellular autophagy inhibition action is reduced, so that autophagy of cancer cells is induced.
CN102872049A Application of gypensapogenin A to anti-tubercle bacillus drugs The invention discloses application of gypensapogenin A to preparation of anti-tubercle bacillus drugs. According to the high tubercle bacillus morbidity and the emergence of mycobacterium tuberculosis multiple-resistant strain, the tubercle bacillus morbidity and mortality are one the rise; and gypensapogenin A has remarkable tubercle bacillus suppression activity and good application prospect. The application of gypensapogenin A to the preparation of the anti-tubercle bacillus drugs is firstly publicized, the skeleton type is brand-new, the tubercle bacillus suppression activity is unexpectedly strong and the possibility of giving any revelation by other compounds does not exist, so that prominent substantive features are provided and a remarkable progress in the prevention and treatment of the tubercle bacillus infection is made at the same time.
WO2009013901A1 Novel compound, method for production of the compound, pharmaceutical composition, anti-tumor agent, and use of the compound [PROBLEMS] To provide a novel anti-tumor agent. [MEANS FOR SOLVING PROBLEMS] Disclosed are: an ester derivative of koningic acid (a compound shown below; wherein R represents an organic group); a pharmaceutical composition comprising at least the compound; and an anti-tumor agent comprising koningic acid or an ester derivative thereof. Koningic acid or an ester derivative thereof can prevent a tumor by administering it to a human body, another mammal or the like in an effective amount. When an ester derivative of koningic acid is used, the ester derivative can particularly reduce erythrocytic toxicity to a low level and therefore produces reduced adverse side effects.
CN1579253A Amino-acid salt drink and amino-acid salt tonic The invention is an amino acid salt beverage and a technology for producing amino acid salt oral liquid, which is based on the theory for detecting the content of amino acid content by chemist fansilake. The formula is: the inventor uses abovementioned theory, uses natrium glutamine to react with nitrite, and eliminates the carcinogen in nitrite.
CN101439022A Method for preparing clindamycin phosphate powder injection raw medicine The invention discloses a preparation method for a clindamycin phosphate powder injection raw medicine which comprises the steps: (a) purification is carried out on a crude product of clindamycin phosphate; (b) crystallization and crystal growth are carried out on filter liquor after the filter liquor is arranged in a crystallization tank; (c) centrifugal separation and washing are carred on crystallization liquor; (d) fast temperature raising and drying are carried out on a clindamycin phosphate wet finished product. The preparation method for the clindamycin phosphate powder injection raw medicine has the advantages of favorable water solubility, uniform crystal form particles, small specific volume, big bulk density, low solvent residue, and the like. The method also simplifies the process operation, and dramatically enhances the product yield.
CN102793711A Application of isoquercitrin and analogue thereof to dipeptidyl peptidase IV (DPP-IV) inhibitor The invention belongs to the technical field of dipeptidyl peptidase IV (DPP-IV) inhibitors, and particularly relates to an application of isoquercitrin and an analogue thereof to a DPP-IV inhibitor. An isoquercitrin preparation can be used for inhibiting the activity of DPP-IV in vitro and lowering the decomposition of in-vivo GLP-1 by DPP-IV, so that the secretion of insulin is promoted indirectly, and toxic and side effects are eliminated. The isoquercitrin and an analogue preparation thereof can be applied to the DPP-IV inhibitor, and can be further used for preparing foods, medicaments or food and medicament compositions for treating and preventing diseases which are relevant to DPP-IV activity abnormity.
US20120115944 Use of carnitine and dihydroquercitin to positively influence the natural pigmentation process A method for positively influencing the natural pigmentation process of skin or appendages thereof includes topically contacting the skin or appendages thereof with a combination of carnitine and/or a derivative thereof with dihydroquercetin and/or a derivative thereof.
CN102784391A IL-23 and its receptor The invention relates to an IL-23 and its receptor. Nucleic acids encoding mammalian, e.g., primate, receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.
WO2006095178A1 Medicament and treatment for herpes simplex A medicament for use in the treatment of viral infections, such as herpes simplex, that are transmitted anterogradely through the nervous system. Viruses, such as herpes simplex, may lie asymptomatically dormant or latent in nerve cell bodies of the CNS, but when reactivated, by whatever cause, are transported anterogradely along nerve cell axons to a surface of the body, where symptoms of the infection arise. A common form of herpes simplex infection lies dormant or latent in the trigeminal nerve ganglion until reactivated by stress, premenstrual tension or a range of other triggers. The herpes simplex virus (HSV) typically travels along trigeminal nerve axons to the lips, where it leads to symptoms such as cold sores. Herpes simplex infections may also take a more serious form in which the virus travels along nerve cells to the area of the eye socket. Here, HSV may cause symptoms such as ulceration of the cornea, with a potential serious effect on a patient's vision. The active ingredient of the medicament is an alkaloid such as colchicine, vinblastine, vincristine, a cytochalasin or derivaties thereof.
US20110319495 Pharmaceutical Composition for Hepatitis Treatment and Applications A pharmaceutical composition for hepatitis treatment, which comprises lucidone as an active ingredient; and a pharmaceutical acceptable carrier. As lucidone is a natural cyclopentenedione, the pharmaceutical composition of present invention has lesser side effects. The present invention is also related to the application of the pharmaceutical composition.
US7109322 Process for the depletion or removal of endotoxins A process for the depletion or removal of endotoxins from preparations containing active ingredients designated for therapeutical use which are obtained from natural sources by genetic engineering and/or biotechnology by treatment with chromatographic material wherein said natural source are lysed, the fractions obtained are optionally centrifuged, filtrated or treated with affinity chromatographic methods; said fractions are preincubated with an aqueous salt solution and detergents, treated with anion exchange material and then washed with another salt solution, and the active ingredients are eluted from the anion exchanger, followed by further purification in a per se known manner.
CN101836975A Application of isopentene group flavonoid compound used as pancreatic lipase inhibitor The invention belongs to the technical field of medicaments, and in particular relates to application of isopentene group flavonoid compound used as a pancreatic lipase inhibitor. The flavonoid compound has the following structural formula and has a chemical name of: (E)-2-(2,4-dihydroxy phenyl)-5,7-dihydroxy-3-(3-methyl-2-butenyl)-6-(3-methy-l-butenyl)-4H-chromene-4-ketone, and can be extracted from artocarpus nitidus. Pancreatic lipase activity tests and experiments of weight loss action in animals prove that the compound has obvious pancreatic lipase inhibitory activity and weight loss action, can be taken as the lead compound for developing novel medicaments for preventing or curing obesity and related metabolic diseases, and also can be used for preparing the medicaments for preventing and curing clinically common multiple obesity and the related metabolic disease.
EP2723722A1 3,5-diamino-6-chloro-n-(n-(4-(4-(2-(hexyl (2,3,4,5,6-pentahydroxyhexyl) amino) ethoxy) phenyl) butyl) carbamimidoyl) pyrazine-2-carboxamide The present invention relates to the compound of the formula: (I), or pharmaceuticaily acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
US20100136141 Hemostatic agent A generally non-acidic hemostatic agent, having a relatively neutral pH comprising a magnesium compound, such as a magnesium chloride, a magnesium sulfate and/or a magnesium acetate based compound. The resultant agent is generally less caustic than previous agents, when using a similar amount of active material.
US8809274 Adhesive hemostatic agent based on porcine atelocollagen and method for production thereof Disclosed is an adhesive hemostatic agent based on non-blood constituents including DOPA, able to strongly adhere to collagen fibers, and which comprises an antifibrinolytic agent in addition to an esterified atelocollagen which is non-immunogenic and may become positively charged thereon such that the adhesive hemostatic agent has no possibility of mediating particular diseases or viral infections (HIV, HCV, HBV, CMV, etc), unlike conventional agents comprising blood constituents, and readily binds to negatively charged platelets at high adhesive strength, thus inducing quick blood coagulation. Also, provided is a method for preparing the same.
CN1927202B Vitamin E nicotinate microcapsule and its preparing process The invention relates vitamin E nicotinate microcapsules, wherein the constituents include vitamin E nicotinate 30-70%, encystation material 10-50%, other pharmaceutically acceptable auxiliary material 0-45%, emulsifying agent 0.1-5%. The invention also relates the process for preparing the vitamin E nicotinate microcapsules.
WO2009004496A3 Bisanthrapyrazoles as anti-cancer agents Disclosed are novel bisanthrapyrazoles that likely act as bisintercalators and topoisomerase Ilα inhibitors. These compounds show potent inhibition of cancer cell growth, and certain bisanthrapyrazoles bind to DNA more tightly than doxorubicin, a known intercalating anti-cancer drug. Molecular modeling techniques are also disclosed that allow one to predict the DNA binding strength of various intercalators.
US7342004 Superoxide dismutase inhibitors There is provided use of a compound of Formula XI: wherein R3 is a sulphamate group and at least of R1 or R2 is a thioether group as disclosed by the present specification, capable of inhibiting steroid sulphatase.
US7015202 Adjust migration of monocytes, lymphocytes or interleukins; controllinginfections The object of the present invention is to provide the use of glycyrrhizin and its derivatives for inhibition of MCP-1 production. The present invention discloses an MCP-1 production inhibition method and pharmaceutical composition for the same comprising administration of glycyrrhizin and its derivatives in an amount effective for said inhibition to mammals in which migration of monocytes or T lymphocytes is increased, or production of IL-10 is increased, and inhibition of said increase is desired.
CN102872113A Application of Houttuynoid A in medicament for treating leukemia The invention discloses application of Houttuynoid A in preparing a medicament for treating leukemia, belongs to the field of medicine, and relates to application of Houttuynoid A in preparing a medicament for treating the leukemia, application of Houttuynoid A in preparing a medicament for suppressing leukemia cell proliferation and application of Houttuynoid A in preparing a medicament for inducing leukemia cell apoptosis. Houttuynoid A is used for treating the leukemia by suppressing leukemia cell proliferation and inducing leukemia cell apoptosis. The use of Houttuynoid A in preparing themedicament for treating the leukemia involved in the invention is disclosed for the first time; the framework type of Houttuynoid A is a brand new framework type; and Houttuynoid A has an unexpectedly high inhibition activity for the leukemia cells.
US7012081 Antiproliferative agents; skin disorders; vision defects; liver and kidney disorders Substituted anthranilamides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of anthranilamides are described.
EP2484355A1 Laminin-332 production stimulating composition Disclosed is a novel composition which has a function of stimulating production of laminin-332. The composition is stable and safe, and can be used routinely. Specifically disclosed is a laminin-332 production stimulating composition which contains one or more compounds selected from the group consisting of D-alanine, D-hydroxyproline, derivatives and/or salts thereof. The composition may be used for the purpose of suppressing and/or improving a skin condition. The skin condition may include, but is not limited to a photoaging, wrinkles, a rough skin, fine wrinkles and a dry skin. The composition may be used for an external preparation for the skin or a food.
CA2178107C Compositions for topical application to skin, hair or nails Compositions for treating skin which contain azole in combination with a lipid ingredient. The compositions attain keratinocyte differentiation and provide additional benefits. Also disclosed is a method of improving or preventing the appearance of wrinkled, flaky, aged, photodamaged skin by applying to skin a composition containing in a cosmetically acceptable vehicle an azole and a lipid ingredient.
CN1896095A Lucid ganoderma sugar peptide, its production and use A ganoderic glycopeptides product, its production and use are disclosed. The product consists of glycopeptides and ganoderic polyose. The process is carried out by culturing fermentative liquid, adding into enzyme, enzyme decomposing, killing enzyme, homogeneous treating, concentrating, depositing by alcohol, dissolving deposit, filtering by membrane and spray drying. It can be used to treat tumor.
CN103356748A Ventilating paste for relieving nasal obstruction The invention a ventilating paste for relieving nasal obstruction. The ventilating paste comprises the following components: camphor, borneol, menthol, methyl salicylate, flos magnoliae, centipeda minima, motherwort and eucalyptus oil. The ventilating paste for relieving the nasal obstruction, which is disclosed by the invention, is an external paste, has aromatic odor and good cooling feeling, can be used for treating nasal obstruction, headache and running nose which are caused by common cold, has the relieving, wound healing promoting and treatment effects on mosquito bite and skin itching, has the advantages of no irritation, no sensitization, mild property, anti-inflammation, antisepsis and blood circulation promotion, can be smelted and inhaled genially by a nose when used for relieving the nasal obstruction and can be directly smeared on an affected part when used for treating the mosquito bite or relieving skin itching.
US20110159108 Germ guard lid and methods for using germ guard lid Described herein is a beverage lid that is itself treated with and/or impregnated with antimicrobial material to prevent the spread of contaminants and methods of making and using the same. The beverage lid can prevent spread of contaminants, including communicable diseases like influenza, the common cold, streptococcus or staphylococcus. For example, when a person carrying germs, like influenza, touches a beverage lid, the antimicrobial properties of the beverage lid can combat any contamination of the beverage lid by the germs. Another person can drink from the beverage lid that is substantially germ free.
CN101974068B Tanshinon IIA crylic acid or sodium salt thereof, preparation method and application thereof The invention discloses a tanshinon IIA crylic acid or sodium salt thereof, a preparation method and application thereof. The tanshinon IIA crylic acid or sodium salt thereof has the following structure described in the specification. The tanshinon IIA crylic acid or sodium salt thereof provides a reliable path for the clinical application of the tanshinon IIA, and makes up the defects of hyperacidity and large stimulation of a sodium tanshinon II asilate injection as a clinical medicament.
WO2013188999A1 Application of inula lineariifolia lactone a in preparation of medicine for treating multiple sclerosis The present invention provides an application of Inula lineariifolia lactone A in the preparation of a medicine for treating rheumatoid arthritis. The Inula lineariifolia lactone A as an active component and a routine medicinal carrier are used to prepare a pharmaceutical composition prepared, wherein the pharmaceutical composition may be a tablet, a dispersible tablet, a lozenge, an orally disintegrating tablet, a sustained release tablet, a capsule, a soft capsule, a dripping pill, a granule, an injection, a powder injection or an aerosol and the like. The structure of the Inula lineariifolia lactone A is shown in a formular (I).
EP0912521B1 Substituted indazole derivatives and their use as inhibitors phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf) The invention relates to compounds of formula (I), and to pharmaceutically acceptable salts thereof, wherein R and R1 are as defined herein. R2 is selected from the group consisting of (Ia), (Ib), (Ic) and (Id). The invention further relates to intermediates for the preparation of the compounds of formula (I), and to pharmaceutical compositions containing, and methods of using, the compounds of formula (I), or pharmaceutically acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal.
CN101536999B Application of 3,5-dimethoxy-4-hydroxy benzaldehyde in ray protection The invention discloses a new use of 3,5-dimethoxy-4-hydroxy benzaldehyde which is an application of 3,5-dimethoxy-4-hydroxy benzaldehyde in alpha-particle ray damage protection. Test proves that, in the test of cell culture in vitro and ray irradiation with alpha-particle ray, the cell of 3,5-dimethoxy-4-hydroxy benzaldehyde is added in the culture system; the clone forming rate after irradiation is obviously higher than that of the cell without adding medicants, and the gene mutation rate caused by irradiation is obviously lower than that of the cell without adding medicants. Therefore, 3,5-dimethoxy-4-hydroxy benzaldehyde can reduce gene group DNA damage and gene mutation caused by ray irradiation and has the effect of irradiation protection.
WO2010097595A1 Compositions for use in cardioplegia comprising esmolol and adenosine The invention related to a composition for use in cardioplegia, said composition comprising (i) esmolol; and (ii) adenosine, wherein in use the concentration of said esmolol is in the range 0.3-1.5mM, and wherein in use the concentration of said adenosine is in the range 0.1-1.5mM. The invention also relates to methods of making and using such compositions.
CN102512432A Pain relieving drug A pain relieving drug is characterized by consisting of the following components according to part by weight: 400g of wool grease, 67g of arbutin and 70ml of gaultherolin. The drug with the formula is convenient to use, and has strong pain relieving efficacy and small stimulation to the skin.
CN103230594A Medicine composition of alpha-glucosidase inhibitor and vitamin B The invention relates to a medicine composition composed of one of a pharmaceutically acceptable dose of alpha-glucosidase inhibitor and active metabolite of salt thereof, one or more of pharmaceutically acceptable doses of vitamin B, and a pharmaceutically acceptable carrier. The invention belongs to the field of medicine. The invention also relates to an application of the composition in preparing diabetes-treating medicines. With a medicine prepared by using the medicine composition provided by the invention, blood sugar can be effectively reduced, and a beneficial effect of substantially controlling diabetes vascular lesion complications is provided. Therefore, the medicine is a more appropriate anti-diabetic medicine.
EP1793006A2 Nucleic acid ligands and improved methods for producing the same The present invention describes methods for the identification and production of nucleic acid ligands to a target molecule based on the SELEX process. The methods may be performed with modified nucleic acids, blended nucleic acids and with separate steps of contacting of the candidate mixture of nucleic acids with target and with nontarget molecules. Included in the invention are methods for the identification and preparation of nucleic acid ligands to thrombin, vascular endothelial growth factor, human neutrophil elastase, caffeine and theophylline and nucleic acid ligands to thrombin identified by the SELEX method.
WO2013165776A1 Anti-obesity properties of pterostilbene We have determined that pterostilbene demonstrates anti-obesity properties. Rats were fed a commercial obesogenic diet supplemented or not with pterostilbene: PT15 (low dose: 15 mg /kg body weight/d) or PT30 (high dose: 30 mg/ kg body weight/d) for 6 weeks. Pterostilbene significantly reduced total adipose tissue mass (15.1 % in the PT15 group; 22.9% in the PT30 group) without changes in food intake. The activities of lipogenic enzymes were reduced in white adipose tissue and liver. Activities of enzymes involved in liver fatty acid oxidation were significantly increased in the PT30 group. Low dose pterostilbene can reduce body fat by reducing lipogenesis in adipose tissue. At the high dose, two mechanisms contribute to reduction in body fat: (1 ) decrease in adipose tissue and liver lipogenesis, and (2) an increase in liver fatty acid oxidation.
EP1429689A4 Rational drug therapy device and methods A method and a system for treating vascular in-stent restenosis that combines two disparate drug delivery systems wherein the two drug systems act in a synergistic fashion to produce maximal therapeutic benefit at a targeted site. Controlled delivery of non-toxic, subthreshold doses of a systemic drug is combined with the localized delivery of a second drug via catheter-mediated stent placement to provide therapeutic benefit. Because each drug acts independently via distinct yet related molecular pathways, full therapeutic benefit can be designed as additives and occurs only at the targeted site.
WO2006115247A1 HIGHLY SELECTIVE Rho-KINASE INHIBITOR Disclosed is a compound which has a highly selective inhibitory effect on Rho-kinase and is useful as a therapeutic agent for diseases including hypertension, pulmonary hypertension, cerebral vasospasm, angina pectoris, heart failure, arteriosclerosis, glaucoma, dysuria, asthma and erectile dysfunction. A homopiperazine derivative represented by the general formula (1), an acid-addition salt thereof or a solvate of the derivative or the salt: wherein R1 represents an amino acid residue; R2 represents a hydrogen atom or an alkyl group; R3 represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a halogen atom, a nitrile group or a hydroxyl group; and R4 represents a hydrogen atom, a halogen atom or a hydroxyl group.
CN103655453A Preparation method of ezetimibe medicine composition The invention relates to a preparation method of an ezetimibe medicine composition. The preparation method comprises the following steps: 1, suspending ezetimibe in a proper solvent to prepare an uniform ezetimibe micron-sized suspension; 2, adding the suspension into a diluent of the medicine composition in a spraying manner and drying to prepare particles and powder of the ezetimibe medicine composition; and 3, preparing the particles and the powder into the ezetimibe medicinal minimum dose unit. Firstly, the medicine is prepared into the micron-sized suspension, granulation is carried out in a one-step granulation manner, the medicine is added into the diluent and finally, the medicinal minimum dose unit is prepared. The preparation method has the benefits that the effect of the preparation method is superior to that of a method in which micronization is carried out after the slightly soluble medicament is separately micronized; and the operation is simple and the large scale production is easy.
EP2112145A1 Chromenone derivatives useful for the treatment of neurodegenerative diseases Compounds of general formula (I) and (II) in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 and R15 have the meanings given in the specification, are useful in the treatment of neurodegenerative disease.
US7105665 Compound for treatment of diarrhea, nervous system disorders such as Alzheimers and asthma in mammals Disclosed are methods for making novel A2B adenosine receptor antagonists having the structure of formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.
CN102389432A Compound antagonist of animal anesthetic and application of compound antagonist The invention discloses a compound antagonist of an animal anesthetic and an application of the compound antagonist, belonging to a medicine composition in the field of veterinarian. Each ml of compound antagonist comprises active ingredients of 0.5-2.0mg of Yohimbine hydrochloride and 0.1-0.4mg of flumazenil hydrochloride. The compound antagonist of the animal anesthetic has a remarkable awakening effect to an anesthetized animal, better effect compared with the single use of the Yohimbine hydrochloride or the flumazenil hydrochloride, is rapid in awakening, has no any adverse effect, is stable in recovery of circulating and breathing mechanisms, and has large safety factor and clinical application safety.
WO2008108630A1 Polymorphic forms of efavirenz The present invention provides novel crystalline forms of Efavirenz, designated Efavirenz form ULT-I and ULT-2 respectively, methods for the preparation of Efavirenz form ULT-I and ULT-2 respectively and the use of Efavirenz form ULT-I and ULT-2 in pharmaceutical applications, in particular in anti-HIV medicaments. The crystalline form of Efavirenz form ULT-I and ULT-2 can be used in combination with other anti-HIV medicaments such as Tenofovir DF and Emtricitabine.
WO2009048073A1 Method of coating granules It is intended to provide a coating method wherein the elution profile of the principle agent from granules containing a physiologically active substance is controlled by coating cores containing the physiologically active substance by spraying thereto a coating solution which contains a water-insoluble polymer, an organic solvent having a boiling point of 50oC or higher and water and in which the content ratio by weight of the organic solvent to the water is about 89/11 to about 50/50.
WO2007110047B1 TERGURIDE/PROTERGURIDE FOR THE TREATMENT OF CHRONIC PAIN (e.g. MIGRAINE) The invention relates to the use of terguride and proterguride for the prophylaxis and/or treatment of chronic pain, such as backaches, headaches, migraines, neuralgia and to pharmaceutical compositions containing terguride and/or proterguride optionally together with an opiate analgesic.
CN101687884B Macrolactone derivatives The present invention relates to a compound of the formula (I), where X and Y independently of one another are OH, O-(C1-C6)-alkyl, NH2 or NH-(C1-C6)-alkyl, or X and Y together form a group -O-, R1 and R2 independently of one another are Cl or H, R3 is H, (C1-C6)-alkyl, C(=O)-(C1-C6)-alkyl or (C1-C6)-alkylene-NH-(C1-C6)-alkyl, and R4 is H, (C1-C6)-alkyl or C(=O)-(C1-C6)-alkyl, or a physiologically acceptable salt thereof, which is formed by the microorganism ST 201196 (DSM 18870), use thereof for the treatment and/or prophylaxis of fungal disorders, medicaments containing a compound of the formula (I), processes for production thereof and the microorganism ST 201196 (DSM 18870).
CN102178664A New application of schizandrol A, schizandrin and schizandrol extract to prevention and treatment of senile dementia The invention belongs to the technical field of medicaments and discloses application of schizandrol A, schizandrin and a schizandrol extract to prevention and treatment of senile dementia. The invention particularly relates to the effect of the schizandrol extract, the schizandrol A and the schizandrin of improving learning memory disorder of dementia mice induced by injecting Abeta1-42 into lateral ventricle and discusses the action mechanism. The result shows that the schizandrol extract, the schizandrol A and the schizandrin can obviously improve working memory disorder and spatial discrimination learning memory disorder of the mice, can improve SOD and GSH-Px activity, reduce MDA content, can increase GSH content and can reduce GGSG content, and shows that the schizandrol extract, the schizandrol A and the schizandrin can eliminate free radicals generated by in vivo oxidation stress through various routes, can inhibit lipid peroxidation and can improve oxidation resistance of an organism so as to improve oxidative stress damage caused by Abeta1-42. The schizandrol extract, the schizandrol A and the schizandrin can be applied to preparing medicaments or health-care food for preventing and treating senile dementia.
CN102920720A Animal compound kanamycin sulfate and coramine injection and preparation method thereof The invention discloses animal compound kanamycin sulfate and coramine injection and a preparation method thereof. The injection consists of kanamycin monosulfate, coramine, dexamethasone sodium phosphate, sodium bisulfite, EDTA (Ethylene Diamine Tetraacetic Acid)-2Na and injection water; double effects and double inhibiting and killing of pathogenic microbes are achieved, the probability of medicament tolerance of the pathogenic microbes is eliminated, the sensitivity of the pathogenic microbes is increased, and the dexamethasone sodium phosphate is used for resisting inflammation and relieving serious inflammatory response; a few medicaments are reasonably proportioned for symptomatically treating severe diseases of pigs and acting on spinal bone marrow in high blood concentration sports, and the injection has the antibacterial and anti-inflammation effect, has quick treatment response, and can be used for treating both symptoms and root causes, reducing the medicament tolerance of the pathogenic microbes and quickening recovery of the pigs; and the injection serving as a compound preparation is convenient to use, and can be used for achieving the treatment effect of a few medicaments in one-time use.
US7198787 Preferentially kill mammary gland cancer cells; obtain cells, exposed to mixture of toxins, monitor cellular response to toxins A method for killing unwanted target cells in a cell population comprising nucleated cells harvested from peripheral blood, or CD-34+ or similar early progenitor cells selected from the above nucleated cells or from bone marrow aspirates, in which method the cell population is in vitro or in vivo exposed to two or more immunotoxins selectively killing the malignant cells, is described. Furthermore the invention relates to the mixture of immunotixins, the use of the mixture and a kit for performing the method.
WO2013136871A1 Oversulfated chondroitin composition The purpose of the present invention is to provide a unique chondroitin sulfate composition containing a squid cartilage extract, which is used in various technical fields such as the field of medicine, the field of health food, the field of functional food, the field of nutritional supplement, and the field of health care (hair care and the like). This purpose can be achieved, for example, by a composition that contains at least 60% by weight of chondroitin sulfates in total, with chondroitin sulfate E (CS-E) being contained in an amount of more than 40% by weight relative to the total chondroitin sulfates and chondroitin sulfates A and C (CS-A and CS-C) being contained in an amount of less than 20% by weight relative to the total chondroitin sulfates. The composition of the present invention is useful for the treatment of symptoms or conditions of various diseases because of improvement of arthralgia and healthiness of joint (production of collagen and hyaluronic acid, and resistance to inflammation by the combination with midkine), bone growth (growth and calcification of osteoblasts, and production of bone morphogenetic protein and osteocalcin), improvement of metabolic syndrome (insulin secretion), improvement of sexual function (muscle strengthening, hair growth and production of testosterone), improvement of skin conditions (production of collagen and hyaluronic acid), and health care (hair care and the like).
US20110077234 Urea Glucokinase Activators The invention provides a compound of general formula (I) wherein the substituents are defined further in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.
US20100204273 Quinoline and Quinazoline Derivatives Having Affinity for 5HT1-Type Receptors Disclosed are methods for use of compounds of formula (I) in the treatment of CNS disorders such as dysthymia, schizophrenia, panic disorder, obsessive compulsive disorder, post-traumatic stress disorder, pain, and memory disorders: wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description.
CN103405458A Application of Chukrasone A in medicaments for treating hepatocellular carcinoma The invention discloses an application of Chukrasone A in preparing medicaments for treating hepatocellular carcinoma, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT(3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluation finds that the Chukrasone A also has a significant inhibitory effect on the growth of human hepatocellular carcinoma cell strains HepG2, MHCC-LM3, Bel-7402 and HuH-7. Therefore, the Chukrasone A can be used for preparing anti-hepatocellular carcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating hepatocellular carcinoma provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to hepatocellular carcinoma cells.
US20120178679 Fused aromatic ptp-ib inhibitors The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
EP1554393A2 P27 prevents cellular migration This invention provides methods of preventing cellular migration and of treating cardiovascular diseases and tumor metastasis by increasing the intracelllular concentration of cyclin-dependent kinase inhibitor p27 or C3 exoenzyme or decreasing the intracellular concentration of Rho-kinase, and methods of identifying chemical compounds for use in such treatments.
WO2009042444A3 Methods and compounds for treating retinol-related diseases Compounds that reduce serum retinol levels are used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods, compounds, and compositions to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions.
CN101687870A Nitrogenous heterocyclic compounds, preparation thereof and use thereof as antibacterial medicaments The invention relates to nitrogenous heterocyclic compounds, the preparation thereof and the use thereof as antibacterial medicaments, the compounds of general formula (I) in which R1 is a (CH2)n-NH2 or (CH2)n-NHR radical, wherein R is a (C1-C6) alkyl and n is equal to 1 or 2; R2 is a hydrogen atom; R3 and R4 together form a nitrogenous heterocycle of aromatic nature with 5 vertices, containing 1, 2 or 3 nitrogen atoms, optionally substituted with one or more R' groups, wherein R' is selected from the group comprising a hydrogen atom and alkyl radicals containing from 1 to 6 carbon atoms, in free form, in the form of zwitterions, and in the form of salts with pharmaceutically acceptable mineral or organic bases and acids.
US7112579 26,27-Homologated-20-EPI-2-alkyl-19-nor-vitamin D compounds This invention provides a novel class of vitamin D related compounds, namely, the 2-alkyl-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 is selected from the group consisting of alkyl, hydroxyalkyl and fluoroalkyl, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds, especially the 2α-methyl and the 2α-methyl-20S derivatives, are characterized by relatively high intestinal calcium transport activity and relatively high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.
CN102048876A Bagged external washing ointment for assisting treatment of gynecologic inflammation and itchiness and preparation method thereof The invention provides a bagged external washing ointment for assisting treatment of gynecologic inflammation and itchiness. The ointment is characterized in that the formula comprises the following raw materials according to weight percentage: 15-35 percent of dandelion, 10-25 percent of sophora flavescens ait, 5-25 percent of common cnidium fruit, 5-25 percent of cortex phellodendri, 15-35 percent of honeysuckle and 3-10 percent of calcined alum. The preparation method comprises the following steps of removing foreign impurities, cleaning, drying, grinding, sieving and bagging. The ointment has the effects of clearing away heat and toxic material, diminishing inflammation, treating urinary tract infection, treating toxic heat, curing leprosy and sore, removing erosion and itchiness of vulva, curing trichomonas vaginitis, eliminating pustules, reducing swelling, curing phlegm and persistent pain, relieving itching, curing trauma infection, relieving prickly heat, astringing, stopping bleeding, growing flesh and the like.
US20080254153 Water Dispersible Composition and Method for Preparing Same The invention pertains to a water dispersible, preferably a powder composition of water extractible bioactive components of exclusively fruit or vegetable or plant origin. These components are obtainable by: a) subjecting a selected fruit or vegetable or plant material to homogenisation in weak alkaline conditions and at moderate temperature; b) separating the liquid extract from the homogenised mass and subsequently bringing it to neutrality; and c) eventually concentrating or drying, preferably by freeze drying, the neutralized liquid extract. The composition can be used as primary composition in the preparation of a food product for oral administration, a food supplement, a pet food product, a pet food supplement, a cosmetic preparation or a pharmaceutical preparation.
US20080207668 Pharmaceutical compositions of hydromorphone for prevention of overdose or abuse The invention relates to compounds, compositions and methods comprised of a chemical moiety attached to hydromorphone. The invention provides embodiments that provide a decrease in the potential of hydromorphone to cause overdose or to be abused while still delivering therapeutic activity similar to that of the parent hydromorphone.
WO2012164535A1 Antioxidant composition for the reduction of the causes of reduced male reproductive capacity The present invention relates to a composition characterised in that it comprises inositol and N-acetyl cysteine. Object of the present invention is also the composition according to the invention for use in the treatment of conditions that cause a reduced male reproductive capacity. The present invention also relates to the use of the composition according to the invention as a dietary supplement.
CN102106915A Liniment for treating psoriasis and preparation method thereof The invention provides liniment for treating psoriasis and a preparation method thereof. The preparation method comprises the following steps of: grinding lightyellow sophora root, gentian root, rhubarb and root-bark of ditlany into powder, and soaking the powder in mature vinegar for one week to prepare filtrate 1; completely dissolving benzoic acid, salicylic acid, camphors and borneols in 75 percent ethanol to prepare solution 2; and mixing the filtrate 1 and the solution 2, and sealing the mixed solution to prepare the liniment. The liniment has the effects of clearing away heat and eliminating dampness, expelling pathogenic wind and relieving itching, killing bacteria and relieving itching and dissolving aging skin, can be used for treating psoriasis and has the characteristics of quick response, low side effect and relapse prevention; and according to clinical observation, the curing rate is 78.1 percent.
US20140227177 Scanning Suspension Comprising a Particle with a Diameter of at least 1 Micrometer The invention provides a scanning suspension comprising a particle which is capable of at least in part disturbing a magnetic field, wherein said particle comprises a diameter of at least 1 μm, and use thereof for obtaining a scanning image. Preferably, said particle comprises holmium and a composition capable of essentially maintaining its structure during irradiation. A particle of the invention is suitable for preparing a kit of parts, comprising a diagnostic and a therapeutic composition which both comprise particles of the invention with essentially the same chemical structure, wherein said therapeutic composition is more radioactive than said diagnostic composition. Said kit of parts is especially suitable for treatment of a tumor. First, the distribution of a particle of the invention within an individual can be determined with a scanning image obtained with said scanning composition. Subsequently, a radioactive therapeutic composition can be administered, wherein a suitable dose of said therapeutic composition is derived from said scanning image.
CA2193627C Subcutaneous implant A non-abusable, non-inflammatory, biocompatible, non-biodegradable, subcutaneous, polymeric implant for the prolonged, controlled release of hydromorphone with near zero-order kinetics is described. Methods of alleviating cancer pain and treating opioid drug addiction with the implant are also described.
US7132433 Use of (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4- piperidinemethanol or its prodrug in the treatment of behavioral or psychological symptoms associated with a disease The present invention is directed to use of (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol or its prodrug depicted as Formula II, wherein R is C1-20alkyl, in treating patients for behavioral or psychological symptoms associated with Alzheimer's disease, Lewy body dementia or Parkinson's disease.
WO2010118015A1 Control of concentric tubing direction An apparatus and a method to control rotational positioning of continuous concentric tubing that extends from a surface downhole in a subterranean well or bore. In one version, a continuous cylindrical inner tube resides within and is concentric with a cylindrical outer tube. At least one elliptical lobe extends from the continuous inner tube. The invention utilizes diameter restrictions within and attached to the outer concentric tubing so that the elliptical lobe or lobes engage the diameter restrictions. Accordingly, rotation of one tube rotates or orients the other tube.
WO2008107211A3 Novel p2y12 receptor antagonists The present invention relates to compounds of Formula (I), in which A and B are independently CH2, O, S, NH, C=O, C=NH, C=S or C=N-OH; X is NH, O, S, C=O or CH2 and R1-R5 are as defined in claim 1, which are P2Y12 receptor antagonists and useful for treating, alleviating and/or preventing diseases and disorders related to P2Y12 receptor function as well as pharmaceutical compositions comprising such compounds and methods for preparing such, compounds. The present invention is further directed to the use of these compounds, alone or in combination with other therapeutic agents, for the alleviation, prevention and/or treatment of diseases and disorders, especially the use as antithrombotic agents for inhibiting platelet aggregation.
CN101579340A Composite medicine preparation for treating gastro-enteritis and gastric ulcer The invention discloses a composite medicine preparation for treating gastro-enteritis and gastric ulcer. The composite preparation comprises the following components: three pieces of berberine of 0.1g, four pieces of furazolidone of 0.1g and three pieces of vitamin B6 of 0.5g. The composite preparation has one course for a week, in the first course, administration is carried out for each day with every four hours, and one course can be effective. In the second course, administration is carried out for each day with every six hours; in the third course, administration is carried out for each day with every 8 hours, then the gastrointestinal diseases of gastro-enteritis, gastric ulcer and the like can be radically treated thoroughly. A patient can not drink wine in the courses. In order to consolidate the curative effect, another course can be added, and in the fourth course, administration is carried out for each day with every 8 hours. The invention can cure the gastrointestinal diseases of stomachache, gastric acid, gastrectasia, diarrhea, stomach heat, stomach cold and the like thoroughly.
US20090318514 Novel Pharmaceutical Compositions The invention provides the use of compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, for the manufacture of a medicament for the treatment or prophylaxis of a condition that may be treated with a thyroid receptor agonist or partial agonist wherein R1, R2, R3, R4, Y, W and R5 are as defined in the specification. The invention also provides compounds of formula (Ia) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, formula (Ia) wherein R1, R2, R3, R4, Y, W and R5 are as defined in the specification.
US20080269268 Substituted Phenylamino-Pyrimidines The invention relates to substituted phenylaminopyrimidines, to a process for their preparation and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases in humans and animals, in particular cardiovascular disorders.
US20100292238 Phenoxymethyl Heterocyclic Compounds Phenoxymethyl compounds that inhibit at least one phosphodiesterase 10 are described as are pharmaceutical compositions containing such compounds an methods for treating various CNS disorders by administering such compounds to a patient in need thereof.
EP1917239A1 Fluoroprostaglandins nitroderivatives Nitroderivatives of fluoroprostaglandins having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
US20080070922 DDPIV inhibitor: selected from (S)-1-{2-[5-cyanopyridin-2yl)amino]ethyl-aminoacetyl)-2-cyano-pyrrolidine, vildagliptin, Sitagliptin, saxagliptin; PDGF receptor tyrosine kinase inhibitor: selected from imatinib, imatinib methanesulfonate; impaired glucose metabolism; impaired glucose tolerance The present invention relates to a combination, comprising; i) DPP IV inhibitor or a pharmaceutically acceptable salt thereof, and ii) at least one PDGF receptor tyrosine kinase inhibitor or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention, delay of progression or treatment of a disease or condition selected from insulin resistance, impaired glucose metabolism (IGT), conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, diabetes particularly type 1 or type 2 diabetes mellitus, obesity, diabetic retinopathy, macular degeneration, cataracts, diabetic nephropathy, glomerulosclerosis, diabetic neuropathy, erectile dysfunction, premenstrual syndrome, coronary heart disease, hypertension, angina pectoris, myocardial infarction, stroke, vascular restenosis, skin and connective tissue disorders, foot ulcerations and ulcerative colitis, endothelial dysfunction and impaired vascular compliance, and vascular events, cardiovascular morbidity or mortality associated with diabetes (e.g. type I or II) or IGT.
US20130034517 Targeted drug phosphorylcholine polymer conjugates The present invention provides random copolymers containing phosphorylcholine and one or more functional agents, and methods of preparing such random copolymers.
EP1652839A2 Drug efflux pump inhibitor A medicament for preventive and/or therapeutic treatment of a microbial infection having an activity of eliminating resistance of a microorganism with acquired resistance to an antimicrobial agent, which comprises as an active ingredient a compound represented by the following general formula (I), a physiologically acceptable salt thereof, or a hydrate thereof: wherein R1 and R2 independently represent hydrogen atom, a halogen atom, carboxyl group and the like; J1 represents a 5- or 6-membered heteroaromatic ring; W1 represents -CH=CH-, -C≡C-, -CH2CH2- and the like; A1 represents phenylene group, pyridinediyl group, furandiyl group and the like; G1 represents oxygen atom, carbonyl group, ethynyl group and the like; p represents an integer of from 0 to 3; G2 represents phenylene group, furandiyl group, tetrahydrofurandiyl group and the like; G3 represents -CH2- or single bond; m and n represent an integer of 0 or 1; and Q1 represents an acidic group.
CN1872078A Biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract A gastrointestinal biologic adherent is proportionally prepared from general arasaponin, adhesive chosen from carbomer, sodium alginate, chitosan, CMC-Na, HPMC K100M, HPMC K15M, HPMC K4M and HPMC 15Lcp, and/or the shifting aid chosen from sodium alginate, CMC-Na, HPMC K100M, HPMC K15M, HPMC K4M, HPMC RT15 and chitosan.
EP2470168A1 Methods for the prevention and treatment of cerebral ischemia The present invention provides methods for the treatment, amelioration, or prevention of a symptom of neuronal damage associated with cerebral ischemia comprising administering compositions comprising a compound of Formula (I).
CN103495018A Method for preparing refreshing Shengmai oral liquid The invention relates to a method for preparing oral liquid and discloses a method for preparing refreshing Shengmai oral liquid, for solving the technical problem that the conventional anti-fatigue oral liquid contains caffeine and has single effect. The method comprises the following steps: 1, preparing a Shengmai drink base solution, namely decocting codonopsis pilosula, ophiopogon japonicus and schisandra chinensis, filtering, mixing the decoction, performing suction filtration, concentrating at normal pressure, cooling, adding absolute ethyl alcohol, concentrating, fixing the volume, thus obtaining the Shengmai drink base solution; and 2, preparing refreshing Shengmai oral liquid, namely taking the Shengmai drink base solution, adding ginseng total saponins, tea polyphenol, taurine, cane sugar, vitamin C and potassium sorbate, fully dissolving, filtering and fixing the volume, thus obtaining the refreshing Shengmai oral liquid. According to the prepared refreshing Shengmai oral liquid, anti-fatigue effects of the Shengmai drink, ginseng total saponins, taurine and tea polyphenol are combined, and the three ingredients do not have antagonism or contain caffeine substances and do not have side effects on the body. The method is applied to the field of preparation of oral liquid.
EP1434624B1 2-amino-6-(2,4,5-substituted-phenyl)-pyridines for use as nitric oxide synthase inhibitors The present invention relates to the compounds 6-[4-(N-methyl-3-azetidinoxy)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, 6-[4-(N, N-dimethylaminomethyl)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, 6-[4-(N-methylaminomethyl)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, 6-[4-(3-azetidinoxy)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine and 6-[4-(2-dimethylamino-ethoxy)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds and to the use of such compounds as nitric oxide synthase inhibitors in the treatment and prevention of central nervous system and other disorders.
WO2006039806A1 Depression of herg k+ channel function in mammalian cells and applications to the control of cancer cells division The use of an HERG channel inhibitor for controlling the proliferation of cancer cells. Examples of such HERG channel inhibitors include dofetilide, cisapride, E-4031 and a siRNA molecule targeting a sequence involved in the expression of an HERG channel. Other ERG channels are also targets for these inhibitors.
CA2649811A1 Triazoloquinazolinone derivatives as inhibitors of checkpoint kinases The instant invention provides for compounds which comprise substituted triazoloquinazolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
US20090105349 alopecia, prostate cancer, livestock growth, acne; use of 4-aryloxybenzonitriles such as 3-Chloro-4-(2-ethylsulfanyl-phenoxy)-benzonitrile or 4-(2,6-Difluoro-phenoxy)-2-trifluoromethyl-benzonitrile The present invention is directed to the discovery of a new class of androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease sebum secretion and to stimulate hair growth.
WO2012159107A1 Inhibition of renal fibrosis The invention provides compositions and methods for inhibiting renal fibrosis.
US7981873 Use within transplantation surgery The present invention is within the field of transplantation surgery. More closely, the present invention relates to use of a clotting preventing agent in the production of a drug for administration in association with transplantation of insulin producing cells in the form of isolated islets to patients with insulin dependent diabetes mellitus, IDDM. The invention is expected to significantly improve the clinical outcome of transplantation of islets of Langerhans.
CN101607014B Ointment for promoting tissue regeneration and restraining sore and preparation method thereof The invention relates to ointment for promoting tissue regeneration and restraining sore and a preparation method thereof. The ointment comprises oleaginous ointment, oil-in-water cream and water-in-oil cream. The ointment can exert curative effect better based on the prior powder, and is more convenient to apply.
WO2013044811A1 Gemcitabine amide derivative and preparation method and use thereof The present invention relates to the field of medical technology, and in particular relates to a kind of gemcitabine amide derivative with a novel structure. The new compounds of the present invention are very active with regard to many tumour cells such as human lung cancer, colon cancer, breast cancer and liver cancer etc., and therefore can be used for preparing anti-tumour drugs. In addition, these compounds also have anti-viral activity. Also disclosed are a preparation method for the compounds, a pharmaceutical composition containing the compounds and the use thereof in preparing drugs against tumours and viruses etc.
EP1189605B1 High molecular weight primary aliphatic alcohols obtained from beeswax and pharmaceutical use thereof The present invention relates to a naturally obtained mixture of higher molecular weight primary aliphatic alcohols which contain 24 to 34 carbon atoms. This invention also relates to the process for obtaining the alcohol mixture by extraction and purification with organic solvents from beeswax without saponification of the beeswax. The alcohol mixture obtained from beeswax has enhanced purity and contains a mixture of alcohols having 24, 26, 27, 28, 29, 30, 32 and 34 carbonatoms. The alcohol mixture is useful in pharmaceutical compositions, foodstuffs and dietary supplements and is effective for lowering cholesterol in LDL-C levels so that it is effective in treating hypercholesterolemia. Consequently the composition may be used to reduce the risk of coronary heart disease, the atherosclerotic process (platelet hyperaggregability, ischemia and thrombosis) and also acts as an anti-inflammatory and anti-thrombotic agent. The composition also possesses neurotrophic properties and is useful for improving male sexual activity.
WO2008024961A1 Dihydropyridazine, tetrahydropyridine, chromanone, and dihydronaphthalenone derivatives as heat-shock protein 90 inhibitors Disclosed are compounds and pharmaceutically acceptable salts of Formula (I), wherein A, Q1, Q2, Q3, R3, and R4 are as defined herein. Compounds of Formula (I) are heat-shock protein 90 (HSP-90) inhibitors, useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
US20120184500 Stevia extract or steviol for hair care This invention relates to the use of an oral composition comprising Stevia extract, steviol precursors, or steviol which enhances the appearance of hair. It further relates methods of improving the appearance of hair by oral administration of an effective amount of Stevia extract, steviol precursors or steviol.
US20080009539 Azo Compounds and Process for Production Thereof A process for the production of an aromatic azo compound having a 2,3-dihydrobenzofuran ring bearing a diazo group at the 5-position of the ring by conducting the diazo coupling of a 2,3-dihydrobenzofuran derivative represented by the general formula (II): [wherein R1 and R2 are each independently C1-6 alkyl; R3 is optionally substituted aryl; and R4, R5 and R6 are each independently hydrogen, C1-6 alkyl, halogeno, C1-6 alkoxy, or C1-6 alkylthio] with a benzenediazonium salt having an electron-withdrawing group at the p- and/or o-position in a mixed solvent composed of water and a polar organic solvent.
US20110021607 Methods and Compositions Relating to Carcinoma Stem Cells MicroRNA markers of breast cancer stem cells (BCSC) are provided herein. The markers are polynucleotides that are differentially expressed in BCSC as compared to normal counterpart cells. Uses of the markers include use as targets for therapeutic intervention; as targets for drug development, and for diagnostic or prognostic methods relating to breast cancer and BCSC cell populations. BCSCs have the phenotype of having lower expression of certain miRNAs compared to normal breast epithelial cells, or to cancer cells that are not cancer stem cells.
CN101555213A Preparation method of N-(phenelyl)-2-hydroxybenzamide The invention belongs to the technical field of medicine and discloses a preparation method of N-(phenelyl)-2-hydroxybenzamide. The method is characterized in that salicylic acid is firstly prepared into salicyloyl chloride and then reacted with 4-ethoxyaniline to obtain N-(phenelyl)-2-hydroxybenzamide. The method has the advantages of few reaction process, mild reaction condition, high yield, fine product purity and low cost which are applicable to industrial production.
CN103156807A Buflomedilhydroc hloride injection and preparation method thereof The invention discloses a buflomedilhydroc hloride injection containing sodium chloride, polyethylene glycol 400 and a phosphatic buffer solution, and a preparation method thereof. The polyethylene glycol 400 is used as a stabilizing gent; the phosphatic buffer solution is used as a pH adjusting agent for adjusting a pH value of the injection to 6.2-6.6. The injection prepared by the method is stable in quality, relevant substances do not increase during a placing process, visible foreign substances are qualified, curative effect is reliable, and side effects are few.
CN102085374A Asarin medical composition, preparation method and application thereof The invention discloses an asarin medical composition which comprises asarin, phospholipid, bile acid and/or salt thereof, and water-soluble polyalcohol. The invention further discloses a preparation method of the medical composition. The invention also provides an oral preparation prepared from the medical composition.
US20110257205 Xanthine derivatives as selective hm74a agonists The present invention relates to compounds which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
US20080124374 Decellularized bone marrow extracellular matrix The invention is directed to compositions comprising decellularized bone marrow extracellular matrix and uses thereof. Methods for repairing or regenerating defective, diseased, damaged or ischemic tissues or organs in a subject, preferably a human, using the decellularized bone marrow extracellular matrix of the invention are also provided. The invention is further directed to a medical device, preferably a stent or an artificial heart, and biocompatible materials, preferably a tissue regeneration scaffold, comprising decellularized bone marrow extracellular matrix for implantation into a subject.
CN101972266A Composition for treating swine infectious atrophic rhinitis and preparation method thereof The invention discloses a composition for treating swine infectious atrophic rhinitis and a preparation method thereof, and aims to provide the composition for treating the swine infectious atrophic rhinitis caused by infection of swine bordetella bronchiseptica and toxigenic pasteurella multocida, which reduces pathogenic medicament resistance and is convenient to use, and the preparation method thereof. The composition comprises the following components in percentage by weight: 5 to 15 percent of sulfamonomethoxine sodium, 1 to 3 percent of lactic acid trimethoprim (TMP1), 3 to 8 percent of ampicillin sodium, 5 percent of sodium carbonate, 5 to 15 percent of sodium bicarbonate and the balance of anhydrous dextrose. By adopting the sulfamonomethoxine sodium and the ampicillin sodium as anti-pathogenic components, the pathogenic microorganism can be effectively killed, the probability of medicament resistance can be reduced, the composition has an effect on secondary bacterial infection, the lactic acid TMP has obvious synergistic effect on the sulfamonomethoxine sodium and the ampicillin sodium, the sodium carbonate can contribute to dissolving the sulfamonomethoxine sodium and the ampicillin sodium, and the sodium bicarbonate relieves the side effect of the sulfamonomethoxine sodium and prevents crystalluria.
CN102784154A Mesalazine enteric coatel tablet and preparation method thereof The invention discloses a mesalazine enteric coatel tablet and a preparation method of the mesalazine enteric coatel tablet. The mesalazine enteric coatel tablet is characterized in that a nanotechnology, an enteric coating technology and a pellet tabletting technology are adopted to reduce the amount of release in the mesalazine enteric coatel tablet, increase the amount of release in a buffer solution, improve the curative effect, prolong the expiration date, guarantee the product quality, and obtain the promising result.
EP1155121B1 Compositions and methods for modulating serum cholesterol Compositions and methods are provided for modulating serum cholesterol in a subject mammal. In one aspect, the invention features novel anti-lipemic drugs that include at least one identified effector of the Low Density Liproprotein (LDL) receptor and at least one identified serum cholesterol inhibitor. In a particular aspect, the drugs include one identified sphingolipid or protein modifying same linked to one identified serum cholesterol inhibitor. Additionally provided are methods for identifying anti-lipemic drugs capable of modulating the LDL receptor and specifically SREBP-1 maturation, including assays designed to identify pharmacoligical drugs capable of stabilizing or reducing serum cholesterol levels in a mammal and particularly a human patient.
EP1997806A1 Pahrmaceutical compositions for prevention and treatment of central nervous system disorders Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.
CN102727474A Application of L-cysteine in preparing medicines used for relieving or neutralizing effect of alcohol and medicines for protecting liver and kidney The invention relates to application of L-cysteine in reducing damages of acetaldehyde oxidation to cells. L-cysteine is applicable to preparation of medicines used for relieving or neutralizing the effect of alcohol, medicines for protecting the liver and medicines for protecting the kidney. The application of L-cysteine in reducing damages of acetaldehyde oxidation to cells in the invention provides theoretical bases for development of novel products used for relieving or neutralizing the effect of alcohol and offers guarantee to drinkers.
CA2138150C 4-amino-n-(4-methyl-4-piperidinyl)-2-methoxybenzamides Piperidinyl substituted benzamides of formula (I) the pharmaceutically acceptable acid addition salts thereof and the stereoisomeric forms thereof, wherein R1 is hydrogen or halo; R2 is halo; R3 is hydrogen or halo; R4 and R5 each independently are hydrogen, C1-4alkyl or haloC1-4alkyl; and the group NR4R5 may also be azido, Alk is C2-4alkanediyl; pharmaceutical compositions containing said compounds of formula (I) as active ingredient; use of said compounds as a medicine; process of preparing said compounds; compounds of formula (I) containing a radioactive isotope; process of marking 5HT2-receptor sites; and process for imaging an organ are disclosed.
EP2014333A1 Use of cooling agents for treatment or prevention of lacrimation or eye burning The present invention relates to the use of one or more cooling agent selected from the groups of terpenes, carboxamides, menthyl esters, menthone glycerol ketals, terpene analogs, furanones, alkyl substituted urea, sulfonamides, phosphine oxides and combinations thereof, for the manufacture of a medicament for treatment or prevention of lacrimation and/or eye burning.
CN103027899A Cephalosporin ester drug particle in non-gel state after meeting water, and preparation method and application of drug particle The invention relates to a cephalosporin ester drug particle in a non-gel state after meeting water, and a preparation method and an application of the drug particle, and belongs to the technical field of pharmaceutical preparations. The drug particle comprises the following raw and auxiliary materials: a cephalosporin ester drug with the bulk density of 0.1-0.3g/ml, and the following auxiliary materials accounting for the mass percentage of the cephalosporin ester drug as follows: 2-4.5% of micropowder silica gel, 2-4.5% of anti-gel adjuvant, and 12-16% of disintegrating agent, wherein the anti-gel adjuvant is a glidant and/or a lubricant with the bulk density greater than 0.50g/ml. According to the cephalosporin ester drug particle in the non-gel state after meeting the water, and the preparation method and the application of the drug particle, the problem that the dissolution rate is relatively low due to the fact that gelatinization is severe when the cephalosporin ester drug is dissolved out in the water in the prior art is solved, the dispersity and the hydrophilicity in a dissolution-out process are good, no gelatinization exists, and the dissolution rate is increased greatly.
CN101766595A Solid preparation with levo-oxiracetam as active component The invention provides a solid preparation with levo-oxiracetam as an active component, relating to an oral preparation of the levo-oxiracetam that is an annular derivant of hydroxyl aminobutyric acid (GABOB). The solid preparation contains the levo-oxiracetam or salt or a purified hydrate thereof shown in the following structure; the chemical name is oxiracetam 4-hydroxy-pyrrolidine-2-ketone-1-acetamide; and the oral solid preparation is prepared by the levo-oxiracetam and accessories that can be accepted in terms of pharmacy through the preparation technology. The levo-oxiracetam which uses a single optical isomer can achieve better curative effect and milder toxic/side-effects than a racemate. The solid preparation of the levo-oxiracetam is safe as well as effective, can be controlled and has stable quality.
US20090029996 Pyridazin-3(2H)-One Derivatives And Their Use As Pde4 Inhibitors The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives, to processes for their preparation and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention and suppression of related pathological conditions, diseases and disorders, in particular asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, topic dermatitis, psoriasis or irritable bowel disease.
WO2007109142A3 M3 muscarinic receptor antagonists for treating tumors The present disclosure provides methods of treating a tumor using M3 mtiscarininc receptor antagonists, such as darifenacin. In some examples, the tumor expresses M3 muscarinic receptors, such as tumors associated with smoking. Also provided are compositions that can be used to practice such methods.
CN102613936A Disinfectant wet wipe and preparation method thereof The invention belongs to the technical field of chemical industry and particularly relates to a disinfectant wet wipe and a preparation method thereof. The disinfectant wet wipe comprises the following components in parts by weight: 150 to 300 parts of wet wipe carrier, 200 to 500 parts of purified water, 0.01 to 0.8 parts of benzalkonium bromide, 0.01 to 0.3 parts of iodopropynyl butylcarbamate (IPBC), 0.01 to 0.8 parts of sodium octaborate tetrahydrate and 0.1 to 0.7 parts of glycerol, wherein the wet wipe carrier is a wood pulp or grass pulp facial tissue or a cotton product. The disinfectant wet wipe can efficiently sterilize, can quickly kill various viruses and bacteria on the surface of a human body or an article when being used for wiping the human body or the article, is non-toxic and harmless to the human body, has the advantages of portability, capability of being stored for a long time, and low price, is applicable to places, such as hotels, restaurants and homes, and is an ideal disinfectant article for the daily use of people who go out and accountants.
CN102018925A Compound preparation for treating arthritis The invention discloses a compound preparation for treating arthritis. Zaocys dhumnade, scorpio, centipede, fructus amomi, rhizoma atractylodis macrocephalae and ibuprofen are used as medicaments, and the weight ratio of the zaocys dhumnade, the scorpio, the centipede, the fructus amomi, the rhizoma atractylodis macrocephalae and the ibuprofen is 2:1:1:1:2:1. The medicaments are made into a preparation which is suitable for oral administration, preferably a capsule preparation. The fructus amomi has the effects of removing dampness, promoting appetite, damping the spleen, stopping diarrhoea, regulating qi and preventing miscarriage; the rhizoma atractylodis macrocephalae has the effects of tonifying the spleen, replenishing qi, eliminating dampness and alleviating water retention; the ibuprofen is a chemical medicament and has the effects of remitting acute diseases and relieving pain; and the medicaments jointly have the effects of expelling wind, removing cold, dredging the channel, remitting acute diseases and relieving pain. The invention has the positive effects of obvious curative effect and rapid action on various types of arthritis treatment.
CN103394072A Paste for treating nucleus of fresh-water nuclear pearl, and preparation method and application thereof The invention relates to a paste for treating nucleuses of nuclear pearls, and a preparation method and application thereof. The paste comprises a paste matrix and medicaments. The preparation method comprises the following steps: 1, taking components other than an aqueous surfactant in the paste matrix, heating the components for complete dissolution to form an oil phase; 2, heating distilled water to 80-90 DEG C, adding the aqueous surfactant to form a water phase; 3, emulsifying; 4, cooling to 40-50 DEG C and adding the medicaments; and 5, cooling to room temperature to obtain the paste. The paste provided by the invention can prolong acting time of the medicaments for the nucleuses, accelerate wound healing of shells producing pearls, promote applying of small particles, realize quickly growth of pearl capsules, increase output of right round pearls, fast heal wounds of shells inserted with nucleuses and reduce mortality of pearl-producing clams. The method provided by the invention is simple, easy for realization, and has substantial effects, high efficiency and wide application prospects.
CN102846430A Health-care eyeshade The invention relates to a health-care eyeshade which comprises a shade body covered on eyes and fixing belts and is characterized in that the shade body comprises an outer shade and dressing bags respectively installed in the outer shade corresponding to the left eye and the right eye. The outer shade is an interlayer bag formed by fixedly connecting a surface layer and an inner layer, and a left gap and a right gap which are used for replacing the dressing bags respectively are arranged at the upper edge of the outer shade. Medicine pasts are arranged on the side of the inner layer clinging to the skin corresponding to the left eye and the right eye respectively. Magnets and/or far infrared coating points are arranged on the side of the inner layer clinging to the skin corresponding to the positions around the left eye and the right eye. The dressing bags can be hot pressing bags, cold pressing bags or medicine dressing bags respectively formed by filling heating dressing, refrigerating dressing or medicine dressing in packing bags. The outer shade can be continuously used for multiple times. Different health-care modes can be achieved by replacing different dressing bags according to needs of users. In addition, the health-care eyeshade has the advantages of being simple in structure, multiple in function, convenient to operate and saving in material.
WO2008074749A9 Indazole derivatives as kinase inhibitors for the treatment of cancer Substituted indazole derivativesof formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).
CN102432605A Kinase inhibitor containing methyl-D3 The invention relates to a kinase inhibitor containing acetyl-D3, which can inhibit the activity of kinase, and in particular relates to BCR-ABL (Breakpoint Cluster Region-Abelson) kinase. The inhibitor provided by the invention has a structure shown in formula (I) in the specification, and can be used for preparing a pharmaceutical composition, namely used for inhibition of kinase in human or animal, such as treatment of tumor and/ or other diseases.
US20110052663 Hemostatic Sponge with Enzyme and Method of Manufacture In one embodiment, a method of making a wound dressing comprises dissolving at least one hemostatic agent in at least one solvent to form a solution. The method continues by freeze drying the solution to form a sponge. The method further comprises including an enzyme in the sponge that enables a human body to readily degrade the hemostatic agent.
EP1685834A1 Use of pinolenic acid for the treatment of obesity Pinolenic acid or a derivative thereof can be used for weight management. The pinolenic acid may, for example, be used in the form of a food supplement, a pharmaceutical composition or a food composition.
US7232821 (2-((2-alkoxy)-phenyl) -cyclopent-1enyl) aromatic carbo and heterocyclic acid and derivatives Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2, Rx, R8, R9 and n are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
US6861439 Treatment of cerebrovascular disease A method of treating a cerebrovascular disease, particularly stroke, is described. A method of treating a cerebrovascular disease includes administering pyridoxal-5′-phosphate, pyridoxal, pyridoxine, pyridoxamine, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxal-4,5-aminal, pyridoxine phosphonate analogues, or pharmaceutical compositions thereof.
EP1680405B1 Bengamide derivatives and use thereof for the treatment of cancer The invention relates to bengamide derivatives which are formed by the micro-organism Myxococcus virescens ST200611 (DSM 15898), during fermentation, to the use thereof for the treatment of cancer, to medicaments containing bengamide derivatives, to a method for the production of bengamides of formula (V), in addition to the micro-organism Myxococcus virescens ST200611 (DSM15898).
EP2493851A2 Closthioamides This invention relates to the field of biologically active compounds and specifically to closthioamides of formula (I) wherein BA and E are as defined herein, pharmaceutical compositions comprising these compounds, and their use as antibiotic, antifungal, and/or cytotoxic agents.
CN103373999A Purine compound, intermediate, preparation method and application thereof The invention discloses a xanthine compound I, wherein R1 is 2-cyanophenyl or hydrogen; R2 is 2-cyanobenzyl; R3 is amino or wherein n=2-4, m=2-3, D is H or NH2 and E is CH2 or NH. A preparation method of the xanthine compound I comprises the following steps of: performing nucleophilic substitution reaction on a compound II and R3H; or (1) performing the nucleophilic substitution reaction on the compound II and R-3-tert-oxyacyl aminopiperidine; and (2) removing a tert-oxyacyl protecting group. The invention further discloses any intermediate of the xanthine compound I, wherein R1 and R2 are as described above. The invention further relates to an application of the xanthine compound I in preparation of a DPP-4 (dipeptidyl peptidase-4) enzyme activity inhibitor or medicaments for treating and/or preventing relevant diseases by inhibiting a DPP-4 enzyme. The xanthine compound I disclosed by the invention provides a new direction for research and development of the DPP-4 inhibitor, and has important significance in development of the potential DPP-4 inhibitors. Formula III, formula II and formula I are shown in the specification.
US20060041019 Inhibitor of anticancer drug side effect An object of the present invention is to provide a novel agent for suppressing side effects of an antitumor agent, which can suppress side effects caused by the use of an antitumor agent, such as hair loss. The present invention provides an agent for suppressing side effects of an antitumor agent which comprises a mixture of cyclic and/or straight chain poly lactic acids having a condensation degree of 3 to 20.
CN1634954A Baicailin derivative, method for preparation and use The invention discloses a baicalin derivative and a preparing method and uses thereof. The provided baicalin derivative is a compound of the general formula (1), wherein at least one of R1, R2, R3, R4 and R5 are selected from the following groups: -OSO3H, -OPO3H2, -Oac, -CH3, -CH3CH2, -CH3CH2CH3 and -CH3CH2CH2CH2 and all of the rest are -OH. The baicalin derivative has a low toxicity, no side effect and has an anti-SARS virus activity.
US20090005340 Bioactive Agents Produced By Submerged Cultivation of a Basidiomycete Cell The invention in one aspect is directed to a method for cultivating a Basidiomycete cell in liquid culture medium, said method comprising the steps of providing a Basidiomycete cell capable of being cultivated in a liquid growth medium, and cultivating the Basidiomycete cell under conditions resulting in the production intracellularly or extracellularly of one or more bioactive agent(s) selected from the group consisting of oligosaccharides, polysaccharides, optionally glycosylated peptides or polypeptides, oligonucleotides, polynucleotides, lipids, fatty acids, fatty acid esters, secondary metabolites such as polyketides, terpenes, steroids, shikimic acids, alkaloids and benzodiazepine, wherein said bioactive agent comprises one or more desirable activities, such as anti-tumour activity, immune stimulating activity, and enhancement of survival of an individual.
WO2011012075A1 Substituted phenyl piperazinyl aralkylone derivatives and its application for preparing analgesic drugs The substituted phenyl piperazinyl aralkylone derivatives shown as the following formula, and the salts and hydrates thereof are disclosed, in which R, R1, R2, R3 and A are defined as the description. The pharmaceutical compositions containing such derivatives and the uses thereof are also disclosed.
DE102010036213A1 Use of peracylated hexoses or peracylated pentoses for improving or normalizing the energy and constructive metabolism of body cells, preferably cells of the central nervous system, muscles and liver Use of peracylated hexoses or peracylated pentoses for improving or normalizing the energy and constructive metabolism of body cells, preferably cells of the central nervous system, muscles and liver, is claimed. - ACTIVITY : None given. - MECHANISM OF ACTION : None given.
CA2846272A1 Pi3k inhibitor for use in the treatment of bone cancer or for preventing metastatic dissemination primary cancer cells into the bone Provided herein are methods for the treatment of bone cancer and prevention of the metastatic spread of cancer.
CN102178657A Novel Olanzapine orally disintegrating tablet The invention relates to a novel Olanzapine orally disintegrating tablet. The tablet comprises (I) a stabilizing Olanzapine coating particulate and (II) an additive, wherein the stabilizing Olanzapine coating particulate contains: (i) a neutral core; (ii) an active layer surrounding the neutral core; and (iii) a protective layer surrounding the active layer. The invention also relates to a preparation method of the stabilizing Olanzapine coating particulate and the novel Olanzapine orally disintegrating tablet containing the stabilizing Olanzapine coating particulate.
US7335772 1H-imidazo [4,5-c] quinolin-4-cyano and 1H-imidazo [4,5-c] quinolin-4-carboxamide intermediates The invention relates to a process for the synthesis of 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo[4,5-C]quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C]quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C]quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-carboxamide, and to the said intermediates.
EP1317432B1 Piperidine derivatives for use as 2,3-oxidosqualene-lanosterol cyclase inhibitors The present invention relates to compound of formula (I), wherein U, V, W, A?1, A2, A3, A4, A5¿, m and n are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
WO2009034547A3 New 4-substituted derivatives of pyrazolo[3,4-d pyrimidine and pyrrolo[2,3-d]pyrimidine and uses thereof The present invention relates to a compound 4-substituted derivative of pyrazolo[3,4- d]pyrimidine or of pyrrolo[2,3-d]pyrimidine having the formula (I) and uses thereof, in particular for the treatment of bone related diseasesand tumours.
CN101385822B Medicine for mainly treating crural ulcer and preparation method thereof The invention discloses a drug for mainly treating leg ulcer. The drug is characterized by being made from the following parts of raw materials by weight: 25-35 parts of yellow lead, 17-23 parts of dragon blood, 13-17 parts of camphor, 17-23 parts of calamine, 13-17 parts of dried alum, 13-17 parts of calcined gypsum, 13-17 parts of ginseng, 13-17 parts of astragalus root, 13-17 parts of Chinese goldthread, 13-17 parts of Chinese teasel root, 13-17 parts of dahurian angelica root, 13-17 parts of manyleaf paris rhizome, 13-17 parts of honeysuckle, 13-17 parts of anomalous wormwood, 13-17 partsof panicled swallowwort root, 17-23 parts of pearl, 17-23 parts of poppy shell, 17-23 parts of pseudo-ginseng, 17-23 parts of cnidium fruit, 17-23 parts of climbing groundsel, 17-23 parts of Chinese lobelia, 17-23 parts of borneol, 17-23 parts of natural indigo and 17-23 parts of leaf of Chinese ilex. The drug has the beneficial effects of good curative effect, convenient use, and simple preparation, and can activate blood circulation to dissipate blood stasis, eliminate necrotic tissues and promote granulation, improve the blood supply of wound surface, cause the granulation to regenerate tissue while expelling rotten materials, and can improve conditions for accelerated wound healing, and has instant effect.
EP2368989A1 Oligoribonucleotide or peptide nucleic acid capable of inhibiting activity of hepatitis c virus The present inventors focused on siE sequences that have been thought to show RNAi activity against HCV viral RNAs, and mainly selected the D5-50 and D5-197 regions present within the IRES region, and carried on the analysis. As a result, the present inventors successfully identified siRNA sequences that exhibit a more effective RNAi activity against hepatitis C virus RNAs. Furthermore, the siRNAs were demonstrated to have a significant inhibitory effect on HCV propagation in an in vivo system.
WO2012130609A1 New combination comprising n-acetyl-l-cysteine and its use The present invention relates to a combination of N-acetyl-L-cysteine, selenium in the form of selenomethionine and melatonin, and a medical product or pharmaceutical composition comprising such combination,useful for the treatment of a variety of diseases and conditions, e.g. benign and malign neoplasia including various types of cancers, autoimmune diseases, neurodegenerative diseases, endocrinological diseases, type 2 diabetes, all types of fibrosis, amyloidosis, endometriosis, polycystic ovary syndrome, dysmenorrhea, dermatological diseases. The combination of N-acetyl-L-cysteine, seleniumin the form of selenomethionine and melatoninis also useful for cosmetic treatment of skin and as an antibacterial agent.
US6858625 Quinolinecarboxylic acid derivative or salts thereof This invention relates to 1-(6-amino-3,5-difluoropyridin-2-yl)-8-bromo-7-(3-ethylaminoazetidin-1-yl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a salt thereof, and also to a medicine containing the same. This compound has characteristic features that, when administered orally, it has extremely high blood half-life and bioavailability while retaining properties that it has extremely high antimicrobial effects and has low toxicity. It can be used widely as preventives, therapeutics and the like for various infectious diseases of human and animals.
CA2414921C Use of diclofenac for treatment of burns The invention relates to the topical use of diclofenac, and topically acceptable salts thereof, (for the manufacture of a topical medicament) for the topical treatment of burns.
CN101757001A Compound slow-release preparation of benorilate, pseudoephedrine and chlorphenamine The invention provides a compound preparation which can comprehensively overcome the symptom relative to cold and can slowly release all the active ingredients. The slow-release preparation of the invention not only can overcome the symptom relative to cold but also can perform the synergistic function of compound medicine. The three active ingredients of the slow-release preparation of the invention can be released and absorbed synchronously so as to acquire expected releasing action in human body. The preparation of the invention can be taken for two times per day, namely, can be taken for one time in morning and evening instead of taking four times per day in the past. The preparation of the invention is characterized by less taking times, slow release in body, stable blood concentration, small fluctuation, high bioavailability and high safety.
US7514567 Oxazolidinone nicotinic acetylcholine receptor agonists Compounds of formula I: and pharmaceutically-acceptable salts thereof, wherein Q, Ar1, A and Ar2 are as defined in the specification, pharmaceutical compositions and formulations containing them, methods of using them to treat diseases and conditions either alone or in combination with other therapeutically-active compounds or substances, processes and intermediates used to prepare them, uses of them as medicaments for therapy, uses of them in the manufacture of medicaments and uses of them for diagnostic and analytic purposes.
CN101007009A A drug for preventing and treating liver injury and lowering blood fat The invention discloses a medicament for preventing and treating liver injury, wherein the effective constituents comprise (by weight ratio) the following raw materials: ferulaic acid 4.5-35.0 parts, red sage root extract 4.9-30.0 parts, and cryptotanshinone 30.0-380.0 parts.
US20110124653 Aryl-sulphonamidic dimers as metalloproteases inhibitors The invention relates to dimeric aryl-sulphonamido compounds endowed with inhibitory activity against metalloproteases MMP, having formula (I) below (M)-L-(M′) (I), wherein M and M′, the same or different from each other, represent the residues of the metalloproteases inhibitors of formula (II), wherein R, R1, R2, R3, G and n have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.
WO2014015167A3 5,5-heteroaromatic anti-infective compounds The invention provides a series of 5,5-heteroaromatic compounds, syntheses thereof, compositions thereof, and methods of using such compounds and compositions. Various embodiments provide methods of killing and/or inhibiting the growth of M. tuberculosis and/or M. avium, and methods of treating, preventing, and/or ameliorating M. tuberculosis and/or M. avium infections in a subject. In various embodiments, the 5,5-heteroaromatic compound is N-(4-(4-chlorophenoxy)benzyl)-2,6-dimethylimidazo[2,1-b]thiazole-5-carboxamide.
US20100113570 Prevention and treatment of post-operative cognitive dysfunction Methods for the use of uncompetitive NMDA receptor antagonist(s) in inhalational anesthesia are provided herein.
US7235535 Method of enhancing drainage of lacrimal system with purinergic receptor agonists A method and preparation for enhancing drainage of lacrimal system in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5′-triphosphate (UTP), dinucleotides, cytidine 5′-triphosphate (CTP), adenosine 5′-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.
EP1511721A2 Guanidino phenylalanin compounds used as urokinase inhibitors The invention relates to the use of derivatives of 3-guanidino phenylalanin as urokinase inhibitors for the treatment of malignant tumors and metastasis.
US8507710 Use of perifosine in combination with antimetabolites for the treatment of benign and malignant oncoses in humans and mammals The invention relates to pharmaceutical compositions comprising alkylphosphocholines and antimetabolite antitumor substances. The pharmaceutical compositions of the invention are useful for the treatment of benign and malignant oncoses in humans and animals. Preferred alkylphosphocholines are described by the Formula II. One such preferred alkylphosphocholine is perifosine.
US6875779 Cyclooxygenase inhibitor The present invention relates to compounds of the formula wherein R1, R3, R5 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).
CN102038791A Refreshing liniment The invention discloses refreshing liniment, which consists of pine needle oil, sodium stearate, lemon oil, dimethyl ether and menthol. The refreshing liniment has a reasonable formula, a good using effect and low production cost.
CN103211975A Red-purple nitrokalite powder for ulcers of lower limbs The invention relates to the field of medicine formulas and specifically relates to red-purple nitrokalite powder for ulcers of lower limbs. The red-purple nitrokalite powder is characterized in that the red-purple nitrokalite powder comprises the following active pharmaceutical ingredients in percentage by weight: 5-8% of bolus rubra, 8-11% of adzuki bean, 10-12% of sinkiang arnebia root, 6-8% of cuttlebone, 8-11% of pomegranate rind, 8-12% of calcined gypsum, 4-6% of common bletilla pseudobulb, 7-10% of abelmoschus manihot, 5-7% of calamine, 0.2-1% of pearl, 2-5% of India madder root, 3-5% of biond magnolia flower, 4-6% of cockscomb flower, 3-5% of puff-ball and 4-6% of agaric, and the 15 active pharmaceutical ingredients are dried, ground to fine powder and screened by a 120-mesh screen to get the powder. The red-purple nitrokalite powder disclosed by the invention has the advantages of low cost, high efficacy in treatment of the ulcers of the lower limbs and no toxicity or side effects, and can clear heat-toxin, promote blood circulation, remove blood stasis, express toxin outward, eliminate slough, promote granulation, disinfect, reduce inflammation, eliminate necrotic tissues, rapidly improve microcirculation of tissues around wounds of the ulcers, increase local blood flow, promote healing of skin ulcer surfaces and prevent recurrence.
EP1713451A1 Solid dosage formulations of galanthamine Galantamine formulations substantially free of microcrystalline cellulose, lactose, and/or starch are described.
US20100144806 Cyclopropanecarboxylic Acid Compound A compound of the formula (I): wherein each symbol is as defined in the description, a salt s thereof, and a prodrug thereof of the present invention unexpectedly have a superior GPR40 receptor agonist activity and superior properties as pharmaceutical products such as stability and the like, and can be safe and useful pharmaceutical agents for the prophylaxis or treatment of GPR40 receptor-related pathology or diseases in mammals.
WO2011024078A1 3 -oxopiperazinium derivatives as agonists of nerve growth factor and their use as medicaments New 3-oxopiperazinium derivatives agonists of Nerve Growth Factor receptors and their use as medicaments. Neurotrophin binding to its specific receptor Trk A leads to the activation of multiple signalling cascades, culminating in neuroregenerative effects, including neuronal survival and neurite outgrowth. Neurotrophic factors have been used for the treatment of several neurodegenerative diseases. However, their use is limited by their inability to cross the blood-brain barrier, their short half life and their side effects. Small molecule neurotrophin peptidomimetics may be beneficial in treating a number of neurodegenerative disorders. The present invention shows the capacity of nerve growth factor agonist molecules derived from the 3- oxopiperazinium scaffold to induce differentiation in PC12 cells and, therefore, that these small molecules with NGF agonist activity may be beneficial for treatment of neurodegenerative diseases, due to their neuroregenerative effects.
US20080050499 Process for preparing a composition comprising steroidal glycosides Process for preparing a composition comprising one or more steroidal glycosides, comprising the steps of: (a) harvesting Hoodia plants, (b) cutting up the harvested plants, (c) drying the cut plants, whereby exposure to UV light during the drying step is avoided, such that the total UV dose is less than about 0.5 kJ/m2 to obtain dried plant material.
US20110086828 Treatment of alcohol abuse and alcoholism using modulators of neurosteroid binding sites on gabaa receptors The present invention provides methods for reducing alcohol drinking behavior in humans and treating acute alcohol poisoning through the use of neutral or negative modulating agents of the neurosteroid sites on GABAA receptors. These agents avoid the unwanted side-effects of opiate antagonists and displays specificity toward the neurosteroid binding sites on GABAA receptors.
CN103211822A Use of sterol derivatives in inhibition of lipase The invention belongs to the field of pharmaceutical engineering and relates to a use of sterol derivatives in inhibition of lipase. The sterol derivatives are compounds shown in the formula I or their pharmaceutically acceptable salts, wherein in the formula I, R1 represents -OH, =O, H, and C1-C3 alkyl; R2 represents -OH, H, and C1-C3 alkyl; R3 represents -OH, =O, H, and C1-C3 alkyl; R4 represents -OH, H and C1-C3 alkyl; and any two or three or four of R1, R2, R3 and R4 simultaneously represent -OH. The sterol derivatives provided by the invention can effectively inhibit lipase. The inhibition effects of the sterol derivatives are in a concentration-effect relationship. The sterol derivatives can be used as drugs or fat-reducing drugs for preventing and/or treating and/or assistantly treating obesity or obesity-related diseases.
US20120022115 Hydroxypyridone derivatives, pharmaceutical compositions thereof, and their therapeutic use for treating proliferative diseases Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
CN101011482A Pharmaceutical compositions for the treatment of acne Disclosed is a pharmaceutical composition for treating acne, which comprises rhubarb horsetails, clove, root of red rooted saliva, citron fruit, red halloysite, baras camphor and momordica seed. The composition has the advantages of low cost, short course of treatment, higher curing rate and low recurrence rate.
WO2006126712A1 Smooth muscle contraction inhibitor Disclosed is a smooth muscle contraction inhibitor, a therapeutic agent and a prophylactic agent for a disease of the circulatory system or a Rho kinase signal transduction system inhibitor comprising at least one substance selected from the group consisting of a docosapentaenoic acid, a salt thereof and an ester thereof. The docosapentaenoic acid is preferably 7, 10, 13,16,19-docosapentaenoic acid and/or 4,7,10,13,16-docosapentaenoic acid. The smooth muscle contraction inhibitor, the therapeutic agent and prophylactic agent for a disease of the circulatory system or the Rho kinase signal transduction system inhibitor can be provided stably and can be used for the inhibition and prevention of the calcium ion-independent smooth muscle contraction without affecting the normal, calcium ion-dependent smooth muscle contraction.
WO2008113051A2 System for treating addictions A system for treating addictions includes genetic testing to determine the presence of allelic variants of genes shown to be associated with impulsive/addictive behaviors and a tailored rehabilitation regimen of specific physical exercise, special diet and particular dietary supplements to optimize the way mood elevation is achieved in the patient. The system further includes individual and group counseling and initial oxygen therapy. The genetic testing assesses the presence of gene polymorphism in at least one of D2 dopamine receptor gene (DRD2), dopamine transporter gene (DATl), dopamine beta-hydroxylase gene (DBH) and serotonin transporter (SERT) gene. The dietary supplements are tailored to stimulate production of neuromediators or neurotransmitters, depending upon the polymorphism determined. The exercises include static and dynamic routines also tailored to the results of the genetic testing. After completion of the inpatient portion of the system, further therapies include daily exercise and dietary supplement programs tailored for each polymorphism discovered.
EP1786817A1 Pteridinones used as plk (polo like kinases) inhibitors The invention relates to compounds of general formula (1), wherein L, Q1, Q2, X, Y, Ra, Rb, Rc, R1, R2, R3, and R4 are defined as indicated in claim 1. Said compounds are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation. Also disclosed is the use of said compounds for producing a medicament having said properties.
WO2009130615A3 Use of deuterium oxide as an elastase inhibitor The invention relates to the use of deuterium oxide (D2O) as an elastase inhibitor and especially as an inhibitor of the human neutrophil elastase (HNE). The invention also relates to the use of deuterium oxide for the prophylaxis and/or treatment of HNE-related diseases.
WO2007007588A1 Compound having cyclic group with planarity as core Disclosed is a compound having aN FXa inhibitory effect, which is useful in the prevention and/or treatment of a thrombotic disease having an activated blood coagulation mechanism, such as a thrombosis/embolism associated with a cardiovascular disease, a thrombosis/embolism associated with a cerebrovascular disease and a thrombosis/embolism associated with a venous disease. A compound represented by the general formula (I), a salt or solvate of the compound or a prodrug of the compound, salt or solvate: (I) wherein the ring A represents a cyclic group having a planarity which may be substituted by a substituent; B represents a cyclic group which may be substituted by a substituent; R1 represents a substituent; and X represents a spacer for the main chain which has 1 to 5 atoms and may be further substituted by a substituent.
CA2124769C Recombinant foamy virus vectors for medicinal and diagnostic uses, and processes for preparing recombinant foamy virus vectors The present invention relates to the preparation of novel vector systems which are generated by in-vitro recombina-tion, using gene technology, of nucleic acids from foamy virus species and of exogenous nucleic acid, and are produced by suitable host cells or by recombinantly altered packaging cell lines. The recombinant preparation of particularly suitable packaging cell lines is likewise a constituent of this invention. The invention is distin-guished by the safe and efficient transfer by foamy virus vectors of therapeutic and other genes into eukaryotic cells.
CN103550213A Omeprazole sodium composition for injection and preparation method thereof The invention relates to injection medicines, and discloses an omeprazole sodium composition for injection. The omeprazole sodium composition comprises the components in parts by weight: 40 parts of omeprazole sodium, 35 parts of mannitol, 3-5 parts of vitamins B6, 3-5 parts of lipoic acid and the proper amount of pH value regulation reagents. The invention also discloses a method for preparing the omeprazole sodium composition for injection. The method comprises the steps: (1) dissolving at first; (2) proportioning liquid; (3) adsorbing and filtering; (4) filling; (5) performing sublimation drying; and (6) processing a finished product. The omeprazole sodium composition has the advantages of high stability and difficulty in color change.
CN103040900A Medicine for treating bedsores The invention belongs to the technical field of medicines, and particularly relates to a medicine for treating bedsores. The medicine for treating the bedsores is definite in curative effect and low in cost. The medicine is prepared by the following raw materials in parts by weight: 10-15 parts of calomelas, 10-15 parts of cinnabar, 30-40 parts of mountain tallow, 10-15 parts of realgar, 10-15 parts of frankincense, 5-7 parts of myrrh, 10-15 parts of white wax, 10-15 parts of fossil fragments and 30-40 parts of calaminae. An appropriate amount of the medicines are smashed respectively and serve as raw materials; the front nine raw materials are mixed and stirred evenly; and then vaseline 250 is compounded, mixed and stirred evenly. The medicine is used for treating the bedsores caused by various acute and chronic diseases, and has a better therapeutical effect.
CN102218122A Quality control and detection method for sea dragon and gecko oral liquid The invention discloses a quality control and detection method for a sea dragon and gecko oral liquid. In the quality control and detection method, on the basis of the original detection standard, a thin-layer chromatography detection method for dried tangerine or orange peel and astragalus root in the prescription of the sea dragon and gecko oral liquid is added, a thin-layer chromatography for ginseng and the astragalus root is improved, and a high performance liquid chromatography for measuring the content of epimedim herb of in the prescription is added. The detection project designed by the invention is reasonable; and the detection method provided by the invention has the advantages of advancement and good accuracy and repeatability, is used for carrying out the quality control on the sea dragon and gecko oral liquid, and can carry out the comprehensive quality control on the sea dragon and gecko oral liquid to ensure the stability and uniformity of product quality.
CA2690191A1 4-carboxybenzylamino derivatives as histone deacetylase inhibitors The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.
CN102049009B Application of pharmaceutical composition containing zedoary turmeric oil and borneol The invention belongs to the technical field of medicines. The invention discloses an application of a pharmaceutical composition using zedoary turmeric oil and borneol as raw materials in preparation of a medicament for treating infertility. Through the pharmaceutical experimental research carried out by scientific researchers, the medicament prepared by using zedoary turmeric oil and borneol asraw materials has a good effect on treating pathological infertility.
WO2010010168A1 Transdermal pharmaceutical compositions comprising danazol The present invention relates to transdermal danazol-containing pharmaceutical compositions, such as gels, and to methods of making and using the same.
US20120004283 Novel shrna gene therapy for treatment of ischemic heart disease Short hairpin RNA (shRNA) interference therapy targeting hypoxia inducible factor—lot (HIF-1 α) prolyl-4-hydroxylase protein (HIF-PHD2) is used for treatment of myocardial ischemia. This treatment can be followed noninvasively by molecular imaging. Provided are compositions comprising novel vectors encoding shRNA targeting the HIF-1α and asparaginyl hydroxylase genes. The vectors encoding shRNA are also useful for the treatment of cardiac diseases, peripheral vascular diseases and decubitis ulcers.
CN103356559A Application of Sarcaboside B in preparation of medicines for treating tongue cancer The invention discloses an application of Sarcaboside B in the preparation of medicines for treating tongue cancer, belonging to the technical field of new applications of medicines. The evaluation on the anti-tumor activity of the Sarcaboside B by an MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method in vitro shows that the Sarcaboside B aslo has an obvious inhibiting effect on the growth of human tongue cancer cell line Tca 8113 and T6. Therefore, the Sarcaboside B can be used for the preparation of the medicines for resisting the tongue cancer and has good development and application prospects. The application of the Sarcaboside B in the preparation of the medicines for treating the tongue cancer is disclosed by the invention for the first time. As the skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpected strong inhibitory activity on tongue cancer cells.
WO2011130383A1 Compounds containing fused rings which inhibit beta-secretase activity and methods of use thereof The invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
EP1905431A1 Pravastatin pharmaceutical formulations and methods of their use The present invention relates to formulations comprising a therapeutically effective amount of pravastatin, or a pharmaceutically acceptable salt thereof, and methods of their use. The present formulations and methods are designed to release little or no pravastatin in the stomach but release a therapeutic amount of pravastatin in the small intestine, thereby limiting systemic exposure of the body to pravastatin and maximizing hepatics-specific absorption of the drug. The formulations and methods of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipids and/or cholesterol in the body.
US20080044411 Human glp-1 mimetibodies, compositions, methods and uses The present invention relates to at least one improved human GLP-1 mimetibody or specified portion or variant, including isolated nucleic acids that encode at least one GLP-1 mimetibody or specified portion or variant, GLP-1 mimetibody or specified portion or variants, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.
CN103070858A Application of benzo Alpha-pyrone compound as Gamma-type human herpes virus-resistant medicine The invention discloses an application of a benzo Alpha-pyrone compound as a Gamma-type human herpes virus-resistant medicine. According to the invention, the compound resistant to Gamma-type human herpes virus infection is higher in activity as compared with a novobiocin which is a marketed medicine, and is less in toxicity based on a cytoxicity test. The compound can be used for curing or preventing related diseases caused by KSHV infection.
CN1839827A Strontium ranelate chewing tablet and its preparation process The invention relates to a chewing tablet containing strontium ranelate as the active ingredient and its preparing process, wherein the tablet comprises 10-90% of strontium ranelate, 9-80% of bulking agent, 0.1-10% of flavoring agent, 0.1-10% of glidant or lubricant, and 0-20% of moistening agent or binding agent. The chewing tablet can be used for treating and preventing osteoporosis.
US20110123482 Methods of Treating Neurological Autoimmune Disorders with Cyclophosphamide Described herein are methods for treating neurological autoimmune disorders in which the treatment method includes administering an immunoablative agent to eliminate most or essentially all maturing and mature elements of the immune system in an affected individual. Following this step, the individual is administered agents to reestablish the ablated immune system.
US20080293770 Psychological disorders; cognition activators Compounds of formula (I) and salts are provided: wherein R5 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; R6 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
WO2006110884A8 2, 6-di (hetero) aryl -4-amido-pyrimidines as adenosine receptor antagonists Compounds of formula (I), including pharmaceutically acceptable salts, esters, solvates and stereoisomers thereof, Rl, R2 and R3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof as antagonists of adenosine receptors, in particular antagonists of the A2A adenosine receptor subtype.
CN103583869A Disease-resistant auxiliary material for chickens and application method thereof The invention discloses a disease-resistant auxiliary material for chickens, which comprises the following active components in unit of weight: wild chrysanthemum flower, lobelia chinensis, immature bitter orange, Mangnolia officinalis, skunk bugbane, Rhizoma Zedoariae, trichosanthes kirilowii Maxim, Bighead Atractylodes Rhizome, herba schizonepetae, Acalypha australis, mung bean, notopterygium root, kudzu root, adamantanamine and sulfadiazine sodium. According to the application method of the disease-resistant auxiliary material for chickens, the weight ratio of the auxiliary material to the feed is (1-1.6):(650-950). The auxiliary material has the advantages of simple proportioning, favorable preventing and treating effects and low medicine residue, and is convenient to use.
CA2363317C Novel process for preparing alendronic acid A novel process for the preparation of alendronic acid is disclosed. The method comprises the steps of reacting a compound of formula (I) with H3PO3 wherein R is an imido group and R1 is selected from the group consisting of chloro, bromo, iodo, fluoro, hydroxy, amino, -OR2 or -OC(O)R2, wherein R2 is C1-C12alkyl, C1-C12 cycloalkyl or C1-C12 aryl; and then reacting the product of the first step with a deprotecting agent. Alendronic acid is then recovered. The method is safe, efficient and suitable for use on a large scale.
WO2012087234A1 A composition comprising at least to compounds which induces indolamine 2,3-dioxygenase (ido), for the treatment of an autoimmune disorder or suffering from immune rejection of organs The invention relates to the use of a composition comprising at least two compounds, each of which induces indolamine 2,3-dioxygenase, for the treatment of an autoimmune disorder or disease or immune rejection of transplants or gene therapeutically modified cells, wherein said inducers have different mechanism of action and wherein the composition gives rise to a synergistic effect on the IDO levels.
WO2009070533A1 Methods of inhibiting steroyl coa desaturase The present invention provides a method of inhibiting a steroyl coA desaturase comprising administering to a mammal in need thereof, a compound of Formula I. The present invention also provides a pharmaceutical composition including a pharmaceutically acceptable excipient and an aliquot amount of a compound of Formula I.
CN102178780A Medicine for treating oral diseases and method for processing same into medicament The invention provides a medicine for treating oral diseases and a method for processing the same into a medicament. The medicine comprises the following raw materials: 3-9 parts of clove, 5-10 parts of dahurian angelica, 15-30 parts of gypsumn, 10-30 parts of fresh rehmannia root, 2-6 parts of coptis root, 3-6 parts of radix sophorae tonkinensis, 6-10 parts of plantain and 6-10 parts of fresh liquorice. The method for processing medicinal materials into a medicament comprises the following steps: (1) soaking the fresh rehmannia root, the gypsumn, the radix sophorae tonkinensis, the plantain and the fresh liquorice in water, and boiling and decocting to obtain dregs and decoction; (2) soaking the clove and the dahurian angelica in water, mixing the soaked clove and dahurian angelica with the dregs obtained in the step (1), and boiling and decocting with water to obtain dregs and decoction; and (3) mixing the decoction obtained in the step (1) with the decoction obtained in the step (2), and adding the coptis root powder to the mixed decoction and mixing to finally obtain the required medicament. By utilizing the method, effective ingredients in the medicament are fully dissolved out, and the mixed medicament of the decoction and the coptis root is obtained finally; and the obtained medicament has obvious curative effect on various oral diseases.
CN102336795A Eucommia ulmoides Oliv active monomer compound and preparation method thereof as well as medicament composition and application thereof The invention discloses a Eucommia ulmoides Oliv active monomer compound of which the structural formula is shown in the specification, and meanwhile discloses a preparation method of the compound, as well as a medicament composition containing the compound and the medicament application thereof. The active monomer compound is extracted from Eucommia ulmoides Oliv or Eucommia bark, Eucommia leaf, Eucommia male flowers or the whole plant of Eucommia ulmoide Oliv. Proven by the experiment research, the extracted active monomer compound 3-((2S,3S,4S,5S))-4,5-dyhydroxy-6-hydroxymethyl-3-((2S,3S,4S,5R)-3,4,5- tripoly hydroxytetrahydrobiopterin-dihydropyran-2-oxygen)-4-oxygen-dihydropyran-2-oxygen)-2-(3,4- dyhydroxy phenyl)-5,7-dioxo-4'-methoxy-isoflavone has a remarkable nervous excitation effect, small side effects, high safety and can be taken for a long time. The invention provides the Eucommia ulmoides Oliv active monomer compound obtained from the Eucommia ulmoides Oliv and the nervous excitation effect of the compound, so as to provide a new natural active substance for the research and development of the novel central nervous system medicament and health food.
EP2044057A2 Derivatives of ureas of piperidine or pyrrolidine, their preparation and their therapeutical use The invention concerns compounds corresponding to formula (I) in which R1a, R1b, R1c, R1d, R2a, R2b, R2c, R2d, R3a, R3b, R4, n, i, j, o, p, q, r and X are as defined in the description. Preparation method and therapeutic use.
WO2013036994A1 Compounds for the treatment of hcv The present invention relates to viral polymerase inhibitors of formula (I), salts, solvates, hydrates, racemates, enatiomers and isomers thereof, in particular inhibitors of viral polymerases within the Flaviviridae family such as hepatitis C virus (HCV), processes for their preparation and their use in the treatment of Flaviviridae viral infection such as Hepatitis C virus (HCV) infections.
US20070298102 Extended Release Pharmaceutical Composition of Celecoxib The invention concerns new pharmaceutical agents comprising the known medicinal celecoxib for oral administration and adapted to release the celecoxib in a controlled manner over an extended period, typically for a period of up 10-12 hours or more. The invention also includes a method for the production of the new pharmaceutical agents and a method for their use to achieve the desirable therapeutic effects of celecoxib, for example in the management of pain.
US7598419 Such as N-(Cyanoacetyl)-3,4-dimethoxybenzylamide Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.
CN102579825A Compound hyacinth bletilla enema The invention relates to a compound hyacinth bletilla enema for treating acute and chronic colitis, ulcerative colitis and ulcerative proctitis. The enema is prepared from the following components in parts by weight: 1-10 parts of berberine hydrochloride, 0.1-3 parts of procaine, 5-35 parts of chlorhexidine acetate, 0.5-5 parts of ephedrine, 1-10 parts of borneol and 10-50 parts of hyacinth bletilla. The enema provided by the invention has the effects of absorbing moisture, arresting bleeding, astringing intestine to correct diarrhea, removing rot muscles to promote tissue regeneration, clearing away heat and alleviating pain, diminishing inflammation, resisting infection and relieving mucosal hyperemia in the intestine, can be used for treating acute and chronic inflammations and ulcers in the recta and colon, and has the advantages of obvious curative effect, high operational convenience, quick effect taking, high safety, no pain and the like. The effective rate is up to 100%.
CN101407515A Chinoline polycyclic compounds as CDK inhibitors The invention provides a quinoline polycyclic compound of general formula I which is used as a CDK inhibitor, and R1, R2, R3 and R4 in the formula are defined in the description. The invention also provides the synthetic route and the preparing method of the compound and the application in treating proliferating diseases of the compound and pharmaceutically acceptable salts of the compound.
US20100145441 Therapeutic agents for angiogenesis-related diseases comprising chondromodulin-i as active ingredient An objective of the present invention is to analyze the function of anti-angiogenic factors in cardiac valves or such to elucidate the developmental mechanism of angiogenesis-induced diseases. A more specific objective is to provide therapeutic agents for angiogenesis-induced diseases such as valvular heart disease, and methods of efficiently screening for the therapeutic agents. The present inventors discovered that chondromodulin-I was markedly expressed in cardiac valves, and plays an important role in maintaining normal functions of the valves by preventing angiogenesis, thickening, and calcification which lead to valvular heart diseases. Chondromodulin-I proteins and substances that activate the expression or function of the proteins are expected to have therapeutic effects against angiogenesis-induced diseases.
US7759338 Programmed cell death, autoimmunity, inflammation, hyperproliferation; easy formulation, shelf life The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.
US20060135599 Use for pharmaceutical composition The invention relates to the use of one or more cannabinoids in the treatment of neuropathic or chronic pain.
CN101792440A Quinazolinone derivatives, preparation and application thereof The invention discloses quinazolinone derivatives, preparation and application thereof, and belongs to the technical fields of medicaments, preparation and application thereof. The application means that the quinazolinone derivatives serve as protein-tyrosine-phosphatase 1B (PTP1B for short) inhibitors. The quinazolinone derivatives are prepared by taking 2-amino-5-iodobenzoic acid or o-aminobenzoic acid as a raw material and performing cyclization reaction on the raw material and 2-methoxyphenylthioisocyanate; and then performing substitution reaction on the reaction product and various halogenated reagents. The derivatives have remarkable PTP1B inhibiting activity, and are particularly suitable to be used as potential anti-diabetic medicaments.
WO2010013925A3 Pharmacological composition for prevention and treatment of respiratory disease containing pyrazolopyrimidinone compound or pharmaceutically acceptable salts thereof Disclosed herein is composition for prevention and treatment of respiratory disease containing a pyrazolopyrimidinone compound or pharmaceutically acceptable salts thereof as an active ingredient.
CN1943743A A medicine for treatment and prevention of vaginitis This invention provides a sort of drug which is used in curing and preventing the woman vaginitis. It has the efficacies of clearing heat and resolving toxin, dislodging damp and killing trichomonas, suppressing bacteria and relieving itching. Specially, the drug is suitable to use in the treatment and the prevention of the vaginitis, the bacterium vaginitis, the mold vaginitis, the dropinsect vaginitis, the non-specificity vaginitis and the vulvapruritus.
US20100196400 Genetic polymorphisms associated with alzheimer's disease, methods of detection and uses thereof The present invention is based on the discovery of genetic polymorphisms that are associated with Alzheimer's Disease. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.
WO2008136850A3 Cobalamin conjugates useful as imaging and therapeutic agents The invention provides detectably labeled cobalamin derivatives which are useful for medical treatment and diagnosis.
CN1907375A Ointment for treating burns and scalds and its preparation Disclosed is a process for preparing ointment for treating burns and scalds, which comprises raw materials of coptis root 20-30g, baikal skullcap root 20-30g, natural indigo 8-12g, garden burnet root 20-30g, rhubarb horsetails 20-30g, calamine 8-12g, prepared rehmannia root 20-30g, calcined gypsum 40-60g, sesame oil 500-600g, medicinal powder 250-300g, and right amount of baras camphor.
US20100022553 Therapeutic Combination Comprising an Aurora Kinase Inhibitor and Imatinib The present invention provides a therapeutic combination comprising (a) a compound 1 of formula (A) as set forth in the specification and (b) a BCR-ABL kinase inhibitor selected from the group consisting of Imatinib, Dasatinib, Nilotinib, Bosutinib and Inno-406, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
CN1875968B Application of anisodamine in preparation of smoking-stopping medicament The invention relates the preparing method for stopping smoking drug with anisodamine. The nicotine reacts with acetylcholine to produce specificity association. The more the nicotine is, the more theacetylcholine is. The anisodamine can effectively oppose the acetylcholine. The anisodamine can also remove free radical, protect cell, accelerate microcirculation flow ratio, and protect body. 5-50mg anisodamine can be mixed with 5% dextrose or 5% dextrose salt solution or 10% dextrose to intravenous inject or intramuscular inject or oral administration. One course of treatment is 10-14 days.
US20090124659 Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase and inhibitors The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.
US20050176745 Based on spiro(1-azabicyclo[2.2.2]octane-3,2'(3'H)-furo[2,3-b]pyridine) ring; ligands for nicotinic acetylcholine receptors; Alzheimer's disease, cognitive or attention disorders, anxiety, depression, smoking cessation, neuroprotection, schizophrenia, analgesia, Tourette's and Parkinson's Compounds of formula I: and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and methods of using such compounds and compositions in therapy.
WO2006076494A1 Catalpic acid for the treatment of type 2 diabetes and associated disorders A method of treating and preventing type 2 diabetes and obesity an animal, including mammals and humans, in which a therapeutically effective amount of catalpic acid to the animal is administered orally or parentally.
US20060083676 For marking and identifying metabotropic glutamate receptor sites and for imaging an organ; in particular non-competitive mGlu1 receptor ligands The present invention is concerned with radiolabelled quinoline and quinolinone derivatives according Formula (I-A)* or (I-B)* showing metabotropic glutamate receptor antagonistic activity, in particular mGlu1 receptor activity, and their preparation; it further relates to compositions comprising them, as well as their use for marking and identifying metabotropic glutamate receptor sites and for imaging an organ. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form —R2—R3—, which represents a bivalent radical of formula -Z4-CH2—CH2—CH2— or -Z4-CH2—CH2— with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula —CH2—CH2—CH2—CH2—; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. Most preferred are radiolabelled compounds in which the radioactive isotope is selected from the group of of 3H, 11C and 18F. The invention also relates to their use in a diagnostic method, in perticular for marking and identifying a mGluR1 receptor in biological material, as well as to their use for imaging an organ, in particular using PET.
EP2036902A2 Urea compounds active as vanilloid receptor antagonist for the treatment of pain Certain compounds of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein R1, R2, P, P', n, p, q, r and s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.
US7115592 antiviral agents for treating HIV-1, HIV-2 or hepatitis B viral infections Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
US20070249564 Novel phosphorus-containing prodrugs Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.
US20050227983 Triazine compounds and their analogs, compositions, and methods The present invention relates to triazine compounds and their analogs and derivatives, and methods and compositions comprising these compounds. The compounds and compositions of this invention are useful for, among other things, treating pathophysiological conditions arising from inflammatory responses, inhibiting or blocking glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells, inhibiting smooth muscle proliferation, treating vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis, and the like.
CN101085302A Apply externally ointment for treating hyperplasia of mammary glands The invention discloses an externally-applied medicinal electuary for treating mammary gland hyperplasia, wherein the active constituents include the following raw material herbs (by weight portion): Chinese angelica root 30, spatholobus stem 30, suakwa vegetable sponge 30, Loranthus mulberry mistletoe 30, eupatene 30, safflower 30, cyperus tuber 30, Ligusticum wallichii 30, capsule of weeping forsythia 30, pericarpium trichosanthis peel 20, rhubarb horsetails 30, mirabilite 30, banksia rose 30, curcuma aromatica 18, milk vetch root 20 and sesame oil 4000.
EP2471782A1 Novel sulfonamide derivative and pharmaceutical product containing same Disclosed is a novel compound which has both angiotensin II receptor antagonist activity and PPARγ activating activity, and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, kidney diseases, arteriosclerosis, inflammatory diseases, type 2 diabetes, diabetic complication, insulin resistant syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. Also disclosed is a pharmaceutical composition which contains the novel compound. Specifically disclosed are: a sulfonamide derivative represented by general formula (I), a salt thereof, or a solvate of the derivative or salt; and a pharmaceutical composition which contains the sulfonamide derivative, a salt thereof, or a solvate of the derivative or salt. (In the formula, R1 represents a C1-6 alkyl group; R2 and R3 each represents a C1-6 alkyl group or the like; and R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-6 alkanoyl group or a C3-8 cycloalkylcarbonyl group.)
WO2009050898A1 Therapeutic agent for colorectal cancer Disclosed is a novel method for treating colorectal cancer. Specifically disclosed is a therapeutic agent for colorectal cancer, which comprises siRNA for AMIGO2 gene or an anti-AMIGO2 antibody or a fragment of the antibody.
EP1724350A1 Method and compositions for the diagnosis and treatment of cancer Methods for the treatment of squamous cell carcinoma using a p53-expressing viral vector are disclosed. In particular embodiments, the vector is a replication-deficient adenovirus. In addition, there are provided methods for examining the development and treatment of microscopic residual disease in the context of post-surgical environments and in body cavities.
EP2296670A1 Glycosaminoglycan oral use and compositions The present invention concerns the use of a glycosaminoglycan association of hyaluronic acid and chondroitin sulfate for the preparation of oral compositions for the prevention or for the treatment of upper gastro-intestinal tract disorders and for the preparation of upper gastro-intestinal epithelial damage, as well as the orale ompositions comprising said glycosaminoglycan association.
US20080275100 For inducing general anesthesia, sedation, and/or hypnotic or sleep effects in patient The invention provides para substituted dialkylphenol derivatives of propofol. The invention further provides pharmaceutical compositions comprising such analogs, methods for preparing such analogs, and methods of using such analogs to induce general anesthesia, sedation, and/or hypnotic or sleep effects in a patient.
WO2012147842A1 Beautiful-skin-promoting agent and use thereof The present invention addresses the problem of providing a beautiful-skin-promoting agent for improving skin conditions such as dry skin, loss of elasticity, and chapped skin and/or for promoting beautiful skin; an oral composition for promoting beautiful skin containing the beautiful skin-promoting agent; and a beautifying method for improving skin condition and/or promoting beautiful skin. Provided is a beautiful skin-promoting agent that contains as an active ingredient one or a combination of two or more types selected from the group consisting of collagen peptides and blood flow-improving agents; especially camellia seed extract, thioctic acids, resveratrols, and plant extracts containing resveratrols, as well as an oral composition containing the beautiful-skin-promoting agent, and a method for oral intake of the beautiful-skin-promoting agent or the composition.
CN102670536A Method for preparing cefixime dispersible tablets The invention discloses a method for preparing cefixime dispersible tablets, relates to the field of pharmaceutical preparation and particularly relates to cefixime dispersible tablets which are anti-infective agents and the method for preparing the cefixime dispersible tablets. Cefixime serves as an active pharmaceutical ingredient of the cefixime dispersible tablets and auxiliary materials are added in the cefixime dispersible tablets. The auxiliary materials include solubilizing agents, filling agents, lubricating agents, bonding agents and disintegrating agents. The cefixime dispersible tablets include, by weight, 15%-60% of the micronized cefixime, 10%-70% of the filling agents or diluents, 1%-20% of the disintegrating agents, 0.3%-5% of the lubricating agents, 0.5%-10% of the bonding agents and 0.5%-5% of the solubilizing agents, wherein grain diameters of the micronized cefixime range from 20 mu m to 120 mu m. The method has the advantages that the dissolving speed of the cefixime dispersible tablets is rapid and the dissolving is complete.
US20100297252 Nanoparticulate meloxicam formulations The present invention is directed to nanoparticulate compositions comprising meloxicam particles having an effective average particle size of less than about 2000 nm.
EP1813283A1 Remedy for neuropathic pain The present invention provides therapeutic agents for neuropathic pain, the agents having excellent therapeutic effects on neuropathic pain, which is an intractable disorder. More specifically, the invention provides therapeutic agents for neuropathic pain comprising, as the active ingredient, an opioid receptor antagonist (particularly naloxone, naltrexone, naloxonazine, naltrindole, etc.), pharmaceutical compositions for treating neuropathic pain comprising an opioid receptor antagonist as the active ingredient, and a method for treating neuropathic pain using opioid receptor antagonists.
CN103479646A Application of Kadcoccitones A to in preparation of anti-helicobacter pylori medicament The invention discloses an application of Kadcoccitones A to in preparation of an anti-helicobacter pylori medicament. The Kadcoccitones A can be applied to treatment of diseases such as acute and chronic gastritis, gastroduodenal ulcer and the like as well as preparation of medicaments for treating acute and chronic gastritis and gastroduodenal ulcer. The Kadcoccitones A belongs to a brand new matrix type, and has high inhibitory activity on helicobacter pylori and the characteristic of outstanding substantiality; meanwhile, the Kadcoccitones A is a significant progress in prevention and treatment of helicobacter pylori infection.
US7659404 Broad spectrum 2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(═O)—, —C(═S)—, —S(═O)2—, C1-6alkanediyl-C(═O)—, C1-6alkanediyl-C(═S)— or C1-6alkanediyl-S(═O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case —A— is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; R5 and —A—R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
EP1261361B1 Oral, nasal and pulmonary dosage formulations of copolymer 1 (glatiramer acetate) Pharmaceutical compositions useful for treating autoimmune diseases in a mammal comprising as an active ingredient a therapeutically effective amount of Copolymer 1, and microcrystalline cellulose are disclosed. Processes for the manufacture of such compositions are also disclosed.
CN101792473A Novel ketolide compound and preparation method and application thereof The invention discloses a ketolide compound similar with the telithromycin antibiotic. The compound has a structural formula as the accompanying drawing. The compound of the invention belongs to a third generation erythromycin analogue antibiotic, has novel structure and stronger activity than the macrolide antibiotic used clinically, has good antibacterial activity on the drug-resistance bacteria by the primary research and has great industrialization prospect.
CN101773475A Preparation method of capsicine micro spheres The invention discloses a preparation method of capsicine micro spheres, which comprises the following steps: (1) dissolving capsicine and carrier materials into an organic solvent to obtain an oil phase according to the mixing ratio of 100 to 250 mg/27 to 100 mg/2 to 5 mL; (2) dissolving emulsifying agents into water as a water phase, wherein the concentration of the emulsifying agents in the water phase is between 5 and 30 mg/mL; and (3) adding the oil phase into the water phase for forming oil-in-water latex emulsion according to the volume ratio of 1/20 to 1/40 under the conditions of the temperature between 20 and 30 DEG C and the stirring speed between 500 and 1200 rpm, continuously stirring the oil-in-water latex emulsion for volatilizing the organic solvent, carrying out centrifugation for collecting micro spheres, washing the micro spheres by distilled water, and preparing the capsicine micro spheres through freeze drying. The capsicine micro spheres prepared by the method of the invention can be made into various slow-release preparations, the stimulation of the capsicine can be reduced, and the medicine concentration can be maintained for a long time, so the medication times can be reduced, the toxic and side effect can be reduced, and the adaptability of patients can be improved.
EP1085804B1 Method and composition for the treatment of epidermal irritations and infections An improved stannous fluoride composition is disclosed. The composition comprises stannous fluoride and at least one zinc containing compound. The zinc containing compounds stabilized and prevent hydrolysis of the stannous ions resulting in a more effective stannous fluoride composition for use in the treatment of epidermal irritations and infections.
WO2014000694A1 Phendioxin heterocycle derivative Provided is a compound of general formula (I) as a potassium channel regulator and pharmaceutically acceptable equivalents thereof. The compound can be used in the preparation of medicines for increasing the ion flow in the potassium channel of mammals or used in the preparation of medicines for the treatment of disease that is sensitive to increasing the ion flow in the potassium channel.
WO2012151346A1 Expression signatures of genes and gene networks associated with skin aging Described herein are expression signatures of genes and coordinately expressed gene networks associated with skin aging, methods used to determine the physiological age of skin, and methods used to screen for compounds used to reduce the visible signs of aging of the skin.
US20100137292 Pharmaceutical formulations of meloxicam This invention is a novel pharmaceutical formulation of aqueous EDTA (Ethylene diamine tetraacetic acid) free solution of meloxicam in combination with meglumin for administration by oral or parenteral route, comprising one or more pharmaceutically acceptable excipients which is comprising N,N dimethylacetamide and propylene glycol for treating mammals, preferably animals.
CN101837002A Anti-cancer sustained-release injection The invention discloses an anti-cancer sustained-release injection. The injection consists of sustained-release microspheres and a solvent, wherein the sustained-release microspheres comprise an anti-cancer active ingredient and a sustained-release auxiliary material; and the solvent is a common solvent or a suspending agent-containing special solvent. The anti-cancer active ingredient is a 5-FU synergist or a combination of 5-FU and 5-FU synergist such as anti-tumor antibiotics, anti-metabolism medicaments, taxane and/or plant alkaloids; the sustained-release auxiliary material is one or a combination of a copolymer (PLGA) of polylactic acid (PLA), polyglycolic acid and glycolic acid, an ethylene vinyl acetate copolymer (EVAc), polifeprosan, and FAD: a sebacic acid polymer; and the suspending agent is one or a combination of sodium carboxymethyl cellulose, mannitol, sorbierite and Tween 80. The sustained-release microspheres also can be prepared into a sustained-release implant, so that systemic toxic reaction of a medicament can be reduced by injecting or placing the sustained-release agent in or around a tumor, local medicament concentration of the tumor can be improved selectively, and the treatment effect of non-operative treatment such as chemotherapeutics, radiotherapy and the like is enhanced.
WO2008036652A3 Amidines as modulators of indoleamine 2,3-dioxygenase The present invention is directed to amidino heterocyclic compounds of formula Ia and IIa which are modulators of indoleamine 2, 3 - dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
CN101264054A Rifamycin sodium injection and preparation thereof The invention relates to a rifamycin sodium injection and the preparation method which enhance the stability of the rifamycin sodium and the quality is stabilized. The invention is characterized in that in every 1000ml injection comprising 35 to 65g rifamycin sodium, 0.1 to 10g vitamin C sodium, 0.1 to 10g glycine, 500 to 900ml organic solvent for injection, the rest is injection water. The production procedure of the injection is: the injection water of proper amount is added into the antioxidant and solution stabilizer for disolving; then the pH value is adjusted; the organic solvent for injection of proper amount is added and blended well; the rifamycin sodium is added and agitated to dissolve and is made rough filteration; and then the solution is filtered by the 0.22 Mum microporous filtering column and is filled into the bottle; then the nitrogen is filled, sealing is made, vapor is circulated, sterilization is continued for 30m; after inspecing and packaging, the injection is obtained.
CN102846547A Gemcitabine or its salt liposome and preparation method thereof The invention relates to gemcitabine or its salt liposome and a preparation method thereof; the liposome comprises gemcitabine or its salts, phospholipid, cholesterol and an emulsifier; the average particle size of gemcitabine or its salts is 10 nm-100 nm. The liposome has higher entrapment efficiency and stability, lower side-effect, and better curative effect.
US20080146594 Thrombopoietin activity modulating compounds and methods Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.
CN102898349A Solid containing compound, a composition containing the solid and use of the solid The invention discloses a solid containing a compound, a composition containing the solid, and a preparation method and a use method of the solid, wherein the compound is (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione. The use method comprises that the solid is used for treating and/or preventing diseases which can be improved by reduction of a TNF-alpha level or by inhibition of phosphodiesterase-4 (PDE4).
US7125885 2-substituted-9-trifluoromethyl-11-methyl-1,2,3,4,5,11-hexahydro-6H-pyrido(3,2-b)carbazole compounds as melanin-concentrating hormone receptor modulators for treatment of G-protein coupled receptor-mediated disorders such as eating disorders, obesity, anxiety disorders and mood disorders The present invention provides compounds having the formula: wherein R1, R2, R, R′ and the subscript p are described herein. The compounds are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. Pharmaceutical compositions and methods of using these compounds for the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor, such as eating disorder, obesity, anxiety disorders and mood disorders are also provided.
CN1682861A Composite medicine for treating diabetes The diabetes-treating composite medicine includes main medicine compounded with orange leaf, sugar and water, and auxiliary medicine compounded with iodine, potassium iodide and water. The main medicine and the auxiliary medicine are packed separately and mixed in certain ratio via shaking before taking. The composite medicine can activate liver fat and restore the function of pancreas, and has the advantages of fast urine glucose reducing speed, stable curative effect, no toxic side effect and no dependence.
CN103690554A Composition and method for killing drug-resistance aspergillus fumigatus The invention provides a composition and a method for killing drug-resistance aspergillus fumigatus, and belongs to the technical field of biology. The method for killing drug-resistance aspergillus fumigatus comprises the following steps: preparing a medicine; collecting a strain; preparing a spore suspension; performing a drug sensitivity test and a combining drug susceptibility test. By virtue of the steps, the minimum inhibitory concentration (MIC) of amphotericin B and cinnamyl aldehyde can be obtained, and the effect of killing drug-resistance aspergillus fumigatus can be achieved by utilizing the medicinal combinations of amphotericin B and cinnamyl aldehyde with different concentrations.
CN103751121A Flucloxacillin sodium freeze-dried powder injection composition and preparation method thereof The invention discloses a flucloxacillin sodium freeze-dried powder injection composition and a preparation method thereof. The composition comprises the following components in parts by weight: 500 parts of flucloxacillin sodium, 10-20 parts of lecithin and 20-40 parts of L-lysine. The preparation method comprises the following steps: (1) dissolving L-lysine and flucloxacillin sodium into water for injection; (2) dissolving lecithin into medicinal ethanol; (3) uniformly mixing the two solutions, filtering the solutions by virtue of a microporous film with the aperture of 0.22 microns, adding the medicinal ethanol into filtrate for volume fixing, adjusting the pH to 5.0 by virtue of a NaOH solution, and performing filling, half tamponade, freeze-drying and tamponade to obtain the flucloxacillin sodium freeze-dried powder injection composition. The flucloxacillin sodium freeze-dried powder injection composition disclosed by the invention is high in stability and easy for realization of industrial production.
US7163933 Treating agent for Paget's disease of bone To obtain a treating agent for Paget's disease of bone, there is provided a method of inhibiting expression of general transcription factor of steroid hormone receptor.
US7357944 Liposomal analgesic drug compositions prepared in GMV using an ammonium sulfate gradient Liposomal bupivacaine compositions are prepared using an ammonium sulfate gradient loading procedure, at a pH which prevents precipitation of the drug from the loading solution. Also described are liposome suspensions comprising ‘GMV’ (giant multivesicular) liposomes and methods for their preparation. The liposomal compositions are characterized by high drug-to-lipid ratios and provide long term analgesia.
US20080247979 Use of a Hydrophobic Zeolite, that Contains and Gives a Slow Release of an Active Element, for Treatment of Skin The invention describes the use of a hydrophobic zeolite, that contains an active component, especially a disinfection element, as ethanol, iodine, phenol, cresol or hydrogen peroxide, in a composition for non-medical treatment of the skin, for example as a deodorant. The invention also describes the use of a hydrophobic zeolite, that contains an active component, especially a disinfection element, as ethanol, iodine, phenol, cresol or hydrogen peroxide, for manufacturing of a pharmaceutical preparation for treatment of skin related conditions and diseases, as skin infections. The hydrophobic zeolite is especially selected from that group that comprises silicalite, or hydrophobic ZMS-5, hydrophobic mordenite and hydrophobic zeolite Y.
CN103239438A Application of kumata kenin in preparation of abnormal vascular proliferation inhibition medicines The invention discloses an application of kumata kenin in preparing abnormal vascular proliferation inhibition medicines. According to the application, kumata kenin serves as an abnormal vascular proliferation inhibitor, and can be used for treating diseases such as cancers, rheumatic arthritis, diabetic blindness and systemic lupus erythematosus which are caused by internal abnormal vascular proliferation. Experiments prove that the kumata kenin has an obvious inhibition function on the abnormal vascular proliferation. Consequently, the kumata kenin can be used for preparing the abnormal vascular proliferation inhibition medicines.
US20090191253 Use of K-252a and Kinase Inhibitors for the Prevention or Treatment of HMGB1-Associated Pathologies The present invention relates to the use of K-252a, a physiologically active substance produced by microorganisms, and of its salts or synthetic and/or chemically modified derivatives for the prevention or treatment of HMGB1 associated pathologies. More particularly, the present invention relates to the use of K-252a for the prevention or treatment of restenosis.
WO2013033520A1 A method for regulating skin pigmentation This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.
CN103083245A Thiamphenicol soluble powder and preparation method thereof The invention relates to a thiamphenicol soluble powder and a preparation method thereof. The thiamphenicol soluble powder mainly comprises the thiamphenicol and pure glucose powder. The preparation method comprises mixing the thiamphenicol and the pure glucose powder according to a certain proportion. The preparation technology uses few auxiliary materials and equipment, is simple in technology, and thus is low in cost and can be easily accepted by the market.
WO2003015783A8 Method of treating alcoholism or alcohol abuse The present invention relates to a method of treating alcoholism or alcohol abuse by administering to a subject a pharmaceutically effective amount of an opioid antagonist before imminent drinking, particularly, by administering said opioid antagonist transmucosally. Preferably, the opioid antagonist used in the method is nalmefene or a pharmaceutically acceptable salt thereof. The invention also relates to a method of treating alcoholism or alcohol abuse by administering to a subject before imminent drinking a transmucosal preparation having rapid onset of action. Advantageously, a FAH+ subject is treated. Further, the invention relates to a method of treating alcoholism or alcohol abuse of a FAH+ subject, comprising extinguishing an alcohol-drinking response by administering to the FAH+ subject a pharmaceutically effective amount of nalmefene or a pharmaceutically acceptable salt thereof.
US20100062081 Use of tellurium containing compounds as nerve protecting agents A novel neuroprotective agent is disclosed for the treatment and prevention of neurodegenerative disorders which is based on the administration of an effective amount of a tellurium compound which has a specific ability to induce the differentiation and interfere with apoptotic cell death pathways of neuronal PC-12 cells.
US20090163599 Mif adsorbant The present invention concerns an apheresis material or adsorbant and a method for removing, depleting or inactivating MIF (macrophage migration inhibitory factor) from blood, blood plasma, blood serum or other body fluids. The present invention is also concerned with the use of said apheresis material or adsorbant. In order to prepare a novel means and novel method, which can reduce the activity or amount of the mediator for sepsis and septic shock, MIF, in a patient's body fluid in a manner which is more pleasant and tolerable for the patient than prior art means and methods, the invention proposes that the apheresis material or adsorbant comprises a solid carrier material on the surface of which MIF-binding molecules or functional groups are immobilized. The method proposes that the apheresis material or adsorbant be brought into contact extracorporeally with the blood, blood plasma, blood serum or other body fluids.
CN102688221A Method for preparing aceclofenac enteric microcapsules Disclosed is a method for preparing aceclofenac enteric microcapsules, comprising dissolving eudragit II, hydroxypropylmethylcellulose phthalate (HPMCP) or cellulose acetate phthalate in acetone to acquire a solution A; then adding aceclofenac powder into the solution A and fully dissolving the aceclofenac powder to obtain a solution B, and acquiring a primary emulsion by placing the solution B in a flask and stirring; adding span 80 into liquid paraffin and fully stirring; adding the primary emulsion into the well-stirred liquid paraffin, heating up to 75 DEG C gradually while stirring, and acquiring microcapsules by stirring continuously while preserving the temperature; and washing the microcapsules by using n-hexane three times after filtering and drying to acquire the finished microcapsules. According to the invention, the aceclofenac slow-release enteric microcapsules are prepared by using a property that decomposition of a capsule wall material is influenced by pH values. Through controlling the capsule wall material, the following effects can be achieved: drugs are sent directionally to the small intestine and released slowly to gentle the plasma concentration, prolong the action time, and improve the curative effect; the dosing frequency can be reduced and the plasma concentration is maintained in the body; and an adverse reaction in the gastrointestinal tract is reduced effectively and patient compliance is also improved effectively.
US20100249168 Compounds and Formulations Suitable for Radical Scavenging The present invention relates to compositions and methods of using free radical scavengers with reduced 1O2 generation. In certain embodiments, these compositions and methods of use relate to fullerene-derived ketolactams and fullerene-derived keto lactam derivatives, fullerene derivatives, and/or fullerenes. In yet other embodiments, the invention relates to cosmetic or dermatological compositions comprising said free radical scavengers with reduced 1O2 generation.
US8263044 Stilbene like compounds as novel HDAC inhibitors The present invention relates to novel stilbene like compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel stilbene like compounds of the general formula (I). Also included is a method for treatment of cancer, psoriasis, proliferative conditions and conditions mediated by HDAC, in a mammal comprising administering an effective amount of a novel compound of formula (I) as described above.
EP1581523B1 Pyrazole-derivatives as factor xa inhibitors The present invention relates to compounds of the formula (I), in which R<0>; R1<1>; R<2>; R<3>; R<4>; Q; V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVlla), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
US20100093700 Methods of Treating Mood Disorders A method of treating at least one symptom or condition associated with but not limited to: Mood Disorders including but not limited to a) Depressive Disorders, including but not limited to, Major Depressive Disorder and Dysthymic Disorder and b) Bipolar Depression and/or Bipolar mania including but not limited to Bipolar I Disorder, including but not limited to those with manic, depressive or mixed episodes, and Bipolar II Disorder, c) Cyclothymic Disorder, and d) Mood Disorder Due to a General Medical Condition, comprising administering an effective amount of formula (I) or its pharmaceutically acceptable salt. In another aspect of the invention a pharmaceutical composition is provided comprising an effective amount of formula (I) or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable carrier or diluent.
EP2707486A1 Diagnosis and treatment of friedreich's ataxia The present invention is directed to oligonucleotides based on peptide nucleic acid oligonucleotide or an equivalent oligonucleotide analogue, such as morpholino or a locked nucleic acid sequences and the use of such oligonucleotides for the dissociation of higher order structures, including triplex-helix DNA structures, in repeated sequences of DNA in Friedreich's ataxia. The dissociation of such structures may be used in the diagnosis and/or treatment of Friedreich's ataxia. Consequently, the present invention is also directed to a method for diagnosing Friedreich's ataxia and the use of peptide nucleic acid oligonucleotide or an equivalent oligonucleotide analogue, such as morpholino or a locked nucleic acid sequences in the treatment of Friedreich's ataxia. Preferably, the oligonucleotides comprise a sequence selected from the group consisting of (GAA)n, (CTT)n, (JTT)n or a mixed (JTT/CTT)n sequence.
CN103340965A External pharmaceutical composition used for treating skin diseases like eczema, dermatitis and tinea and preparation method thereof The invention discloses an external pharmaceutical composition used for treating skin diseases like eczema, dermatitis and tinea and a preparation method thereof. The pharmaceutical composition comprises, by weight, 10 to 100 parts of amur cork-tree bark, 5 to 60 parts of coptis, 5 to 60 parts of natural indigo, 3 to 60 parts of calamine, 3 to 60 parts of dried alum, 1 to 80 parts of artificial cow-bezoar, 2 to 20 parts of borneol and 0.5 to 10 parts of muschus. The invention further discloses a preparation method for an ointment, a gel, a lotion and a cream of the external pharmaceutical composition. The external pharmaceutical composition has a reasonable formula, exerts the effects of heat clearing, detoxifying, dampness eliminating, itching relieving, necrotic tissue removing and tissue regeneration promoting and is applicable to treatment of the skin diseases like eczema, dermatitis and tinea. The preparation method is simple, easy to operate and suitable for industrial production.
US20100261711 Selective anticonvulsant agents and their uses In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of seizures. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of seizures with reduced sedative and ataxic side effects.
EP0923582B1 Substituted 6,5-hetero-bicyclic derivatives This invention relates to compounds of formula (I), wherein the dashed lines represent optional double bonds; A is nitrogen or CR7; B is -NR?1R2, -CR1R2R10-C(=CR2R11)R1, -NHCR1R2R10, -OCR1R2R10, -SCR1R2R10, -CR2R10NHR1, -CR2R10OR1, -CR2R10SR1¿ or -COR2; J and K are each independently nitrogen or carbon and both J and K are not nitrogens; D and E are each selected, independently, from nitrogen, CR4, C=O, C=S, sulfur, oxygen, CR?4R6 and NR8¿; G is nitrogen or carbon; and their use for the prevention or inhibition of a disorder that can be treated by antagonizing CRF.
CN102028644A Bathing article based on medicinal property of related extraction parts of mugwort The invention discloses a bathing article based on the medicinal property of related extraction parts of mugwort, which belongs to the field of healthcare daily articles, and relates to the use, preparation methods and using methods of pet deodorizing and parasite-expelling dry cleaning powder mainly comprising the related components of the mugwort, daily bacteriostatic bathing articles compatible with the mugwort and the like. The pet deodorizing and parasite-expelling dry cleaning powder can expel and prevent parasites from growing on pets, clean the hair of animals and eliminate peculiar smell on pet bodies. Bath foam, liquid soap and the like prepared from the related extraction parts of the mugwort can serve as the daily bacteriostatic bathing articles; and bacteriostatic natural lotion prepared from the mugwort, sessile stemona root and lightyellow sophora root can serve as female bacteriostatic healthcare bathing articles.
CN1732938A Orally integrating tablet of compound paracetamol Disclosed is an orally integrating tablet of compound paracetamol, which comprises 10-40 wt% of paracetamol, 0.5-5 wt% of d-pesudoephedrine hydrochloride, 0.25-2 wt% of dextromethorphan hydrobromide, 0.1-1 wt% of chlorpheniramine maleate, 5-65 wt% of bulking agent, 10-30 wt% of disintegrating agent, 1-20 wt% of flavorings, 5-20 wt% of sweetener, 0.5-3 wt% of flavouring essence, and 0.5-5 wt% of lubricating agent.
US20080207633 Conjugated to polyoxyethylene glycol; analgesics; antidiabetic agents; anticancer agents; sleep disorders; antidepressants; anxiolytic agents Urea derivatives which comprise piperidine or piperazine rings and further substitution are effective in ameliorating conditions characterized by unwanted calcium ion channel activity.
WO2007129729A1 Process for production of fish-derived ceramide, and ceramide-containing composition Disclosed are: a ceramide derived from a vertebrate; a ceramide-containing composition; and a process for production of the ceramide or the composition. The process for producing a ceramide comprises the step of treating a part or the whole body of a fish. The ceramide comprises a ceramide having a d19:3 sphingoid and a C24:1 fatty acid bound to each other through an acid amide bond.
US20080139578 e.g. 1-(3,3-diphenylpropanoyl)piperazine; analgesic: arthritis, headache, migraine, trigeminal neuralgia, allodynia, itch, neuropathic pain, neuralgia, diabetic neuropathy, fibromyalgia, sciatica, back pain; anticonvulsant: epilepsy; Complete Freund's Adjuvant and Capsaicin-Induced Allodynia Models The present invention is directed to the use of substituted piperizine compounds represented by Formula I, for the treatment of pain, including acute pain, chronic pain, cancer pain, visceral pain, inflammatory pain, neuropathic pain, post-herpetic neuralgia, diabetic neuropathy, trigeminal neuralgia, migraine, and fibromyalgia.
WO2011001954A1 Therapeutic agent for abnormal defecation in inflammatory bowel disease patient who is in remission phase A therapeutic agent for abnormal defecation in an inflammatory bowel disease patient who is in the remission phase, which comprises ramosetron, alosetron or a pharmaceutically acceptable salt thereof as an active ingredient.
US20070286863 CMKLR regulation of adipogenesis and adipocyte metabolic function Methods are provided for regulating adipogenesis and metabolic function in adipocytes by modulating the activity of chemokine-like receptor 1 (CMKLR1). Exemplary agents include those that modulate binding of CMKLR1 to a cognate ligand (e.g., chemerin), those that modulate signaling from CMKLR1, and those that modulate expression of either CMKLR1 or its cognate ligand in target cells. Methods are also provided for screening for agents that find use in regulating fat accumulation in a subject.
WO2009134877A3 Therapeutics for treatment resistant mental disorders Described herein are treatments for patients suffering from a mental disorders that include administering an effective amount of an alkylamine-catechol derivative, a quinoline derivative, a bis-quinoline derivative, or combinations thereof.
US20080188415 Composition of matter containing harmonized hydroxyl modified fullerene substance The present invention provides a composition of matter having a harmonized form (Φ/φ) of a hydroxyl modified fullerene having a molecular formula of C60(OH)xHy∀z (where x is from 10 to 36, and y is from 0 to 24 and z is from 0 to 12) the composition of matter having substantially the same 13C NMR spectra shown in FIG. 8 having a dominant peak at 170.2 ppm. This peak shows that each carbon atom of C60 is equally covered by OH groups and that the system [C60(OH)xHy∀z](Φ/φ is one body entity.
US20080255181 Podocytopenia; N-(3-[2-chlorophenyl]-propyl)-R- alpha -methyl-3-methoxybenzylamine; modulate the calcium sensing receptor The present invention relates to methods for treating or preventing podocyte-related diseases and disorders using compounds that modulate the calcium sensing receptor or pharmaceutical compositions comprising thereof.
CN1978452A New process for preparing isoquercitrin This invention uses leaves of Poacynum hendersonii (Hook.F.) Woodson or apocynum venetum Linn as raw material, it utilizes the method of decoction and alcohol sedimentation to remove impurity. After extract is separated by macroporous adsorptive resins, then use polydextran gel LH-20 to purify, obtain isoquercitrin. Compared with the method of traditional silica gel column chromatography, this method has characteristics such as: experiment period is short, dissipation of organic dissolvent is little, yield of produced product is high, and purity coefficient is fine and so on. Isoquercitrin produced by this invention can be provided for medicine research or used as chemistry control article. Through spectrographical identification, isoquercitrin prepared by this invention is ascertained that its structure is meletin-3-O- beta-D-glucopyranose, its purity is determined by purity angle which is less than purity threshold. Purity of this compound is above 99 percent through computation, corresponding to requirement of control article.
US20090264507 Method of diagnosing gum disease-wound healing using single nucleotide polymorphism profiles The present invention provides methods for diagnosing and providing a prognosis for wound healing in a patient by characterizing and analyzing the single nucleotide polymorphism (SNP) of a wound healing associated gene wit3.0. In particular, the invention provides a method of diagnosis and prognosis of oral disease-wound healing, including gingival periodontitis and residual alveolar bone resorption, by characterizing and analyzing the wound inducible transcript-3.0 (wit3.0)SNP pattern in a sample of a patient with and without susceptibility for the disease.
CN101269043A Nicardipine hydrochloride sustained-release dropping pill and preparation method thereof The invention discloses a pharmaceutical preparation for treating primary hypertension, cerebrovascular diseases (such as cerebral arteriosclerosis, cerebral thrombosis and sequela of cerebral hemorrhage), coronary heart disease and anginas of various types, and particularly relates to a prepared sustained-release oral formulation adopting nicardipine hydrochloride as the ingredient. The pharmaceutical preparation aims to supplement the deficiency of the prior art and provide a sustained-release a sustained-release nicardipine hydrochloride dropping pill. The sustained-release nicardipine hydrochloride dropping pill overcomes the defects in the prior art effectively, guarantees no occurrence of an obvious quality change for the drug during the effective storage period and has the advantages of controllable release time, full release and high bioavailability simultaneously.
CN102670582A Inhibitory activity of norathyriol to protein tyrosine phosphatase 1B (PTP1B) and application thereof The invention relates to inhibitory activity of norathyriol to protein tyrosine phosphatase 1B (PTP1B) and application thereof. The invention belongs to the technical field of biological pharmacy, and particularly relates to measurement of inhibitory activity of norathyriol to the protein tyrosine phosphatase 1B, improvement of norathyriol on insulin resistance, and the application of norathyriol in medicaments for treating diseases relative to the PTP1B. An in vitro enzyme inhibition experiment proves that norathyriol is a competitive inhibitor of recombinant humanized protein tyrosine phosphatase 1B, and the IC50 value is 9.2 mu M; and norathyriol can obviously improve the sensitivity of a C57BL/6 normal mouse and an ob/ob diabetic model mouse to insulin, and reduce the blood sugar of experimental animals. Therefore, norathyriol is a novel inhibitor of PTP1B, can be used as a potential lead compound, and is applied to preparation of medicaments for treating metabolic syndromes such as insulin resistance related anti-diabetic metabolic syndrome and adiposis, as well as tumors and other diseases related to the PTP1B.
US20120195932 Geodate delivery vehicles The present invention provides geodate delivery vehicles and methods of manufacture and administration. A vehicle including a lipid monolayer disposed about a hydrophobic domain is disclosed, that can be part of an emulsion or other mixture, or further disposed in a lipid strata. A vehicle including a lipid strata disposed about a hydrophobic domain is also disclosed. The vehicle can be incorporated into a variety of medicinal, food preparations, and personal care products to deliver or stabilize a cargo moiety. Packaged delivery vehicles for to later addition of cargo moieties are also contemplated.
US20090227642 Novel alpha-(n-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production The present invention provides a method for the treatment of head trauma, traumatic brain injury, and/or dementia pugilistica comprising administering a therapeutically effective amount of (2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide.
CN101244042A Folic acid freeze-dried injection and preparation thereof The invention provides a folic acid lyophiled powder injection and a preparation method, comprising folic acid and mannitol. The invention is characterized in that the weight ratio of the folic acid and the mannitol is 1:2.5 to 10. The preparation method has the advantages of simple prescription, little side effect, adopting an advanced freeze drying craft, and plump appearance, good double solubility and fine quality for the prepared product.
EP2424351A1 Anti-cancer drugs, and uses relating for malignant melanoma and other cancers Selenopheno triazene analogs, their compositions, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts and mixtures thereof are useful for the treatment of metastatic malignant melanoma and other cancers. The selenopheno triazene analogs have the general formulae (I) or (II): wherein the substituents R1, R2, R3, R6, and R7 are as described in the specification. Other cancers include which may be treated with these compounds include, but are not limited to, malignant melanoma, leukemia, lymphomas (Hodgkins and non-Hodgkins), sarcomas (Ewing's sarcoma), brain tumors, central nervous system (CNS) metastases, gliomas, carcinomas such as breast cancer, prostate cancer, lung cancer (small cell and non-small cell), colon cancer, pancreatic cancer, Head and Neck cancers and oropharyngeal squamous cell carcinoma.
US20050154007 Substituted imidazo[1,2-a]pyridines such as 2,3-dimethyl-8-(2,6-dimethylbenzylamino)-6-methoxyimidazo[1,2-a]pyridine, used as antisectory agents for prophylaxis of gastrointestinal disorders The present invention relates to novel compounds, and therapeutically acceptable salts thereof of the formula (I), which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.
US20110054001 Chk1 suppresses a caspase-2 apoptotic response to dna damage that bypasses p53, bcl-2 and caspase-3 The invention describes methods that are useful for treating cancer by administering a Chk1 inhibitor which can induce apoptosis in p53-defective cells when combined with a chemotherapy and/or radiotherapy. Methods for screening candidates for a Chk1 inhibitor-based cancer treatment regimen are also described.
US20110059051 Molecular Control of Brown Fat Differentiation and Engergy Expenditure The invention provides methods and compositions for inducing brown fat cell differentiation through modulation of Prdm 16 activity or expression. Also provided are methods for preventing or treating obesity or an obesity related disorder in a subject through stimulation of Prdm 16 expression or activity. Further provided are methods for identifying compounds that are capable of modulating Prdm 16 expression or activity.
EP2367548A1 Medical dietary composition for treating neurodegenerative diseases Medical dietary composition for treating neurodegenerative diseases such as Alzheimer, Parkinson's disease, and more preferably adrenoleukodystrophy comprising a mixture of glyceryl trioleate (GTO), glyceryl trierucate (GTE) and at least one conjugated linoleic acid as active ingredient, in combination with suitable excipients and/or diluents.
US20090054530 Methods and Compositions that Enhance Bioavailability of Coenzyme-Q10 Bioavailability of Coenzyme-Q 10 (“Co-Q10”), an oil-soluble substance, can be enhanced in a subject by modifying, e.g. nanonizing or charging, the form of Co-Q10. Co-Q10 bioavailability also can be enhanced by administering Co-Q10 to the subject as an oil (lipid)-based and water (hydro)-based mixed composition, along with other optional components, such as oils, resins and other carriers. Accordingly, the invention provides various Co-Q10 compositions, e.g. compositions comprised of (i) Co-Q10 dissolved in one or more Co-Q10-soluble oils and (ii) Co-Q10 in admixture with at least one water-dispersible agent. A Co-Q10 complex of the invention, therefore, yields an increased cell absorption rate, as well as an enhanced percentage of Co-Q10 peak absorption, compared to previously known compounds. Methods for making and using the aforementioned compositions also are provided.
WO2006076442A2 Triazolopyrimidine derivatives The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.
CN101040861A Anticancer compound including phosphatidylinostitol 3-kinase inhibitor and alkylate agent The invention relates to an anti-cancer compound as a slow release injection which contains phosphoinositide 3-kinase restrainer and/or alkyl agent, formed by slow release micro ball and solvent. The slow release micro ball comprises the anti-cancer effective components and slow release findings, selected from phosphoinositide 3-kinase restrainer and/or alkyl agent, the solvent is a common solvent or a special solvent with suspending agent, while the viscosity of suspending agent is 100cp-3000cp (at 20-30Deg. C), selected from carboxymethyl cellulose, the slow release finding is selected from phosphate polyester as p (LAEG-EOP), p (DAPG-EOP), p (BHET-EOP/TC), p (BHET-EOP/TC), p (BHDPT-EOP/TC), p (BHDPT-EOP/TC), p (CHDM-HOP) or p (CHDM-EOP), or the polyester or mixture of phosphate and polylactic acid, polyphenyl, 2-aliphatic acid, sebacic acid polyester, poly (erucic acid dimmer-sebacic acid) or poly (fumaric acid-sebacic acid). The anti-cancer compound can be made as slow release plant agent, to inject into cancer or around cancer to hold the effective drug density for more than 60 days, while it can significantly reduce the general reaction of drug and selectively strengthen the effect of non-surgery treatments as chemotherapy or the like.
US20090215773 Dihydropyridine derivatives The present invention relates to dihydropyridine derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, phenyl, (1-5C)heteroaryl R2, R3 are independently (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkoxy, (24C)alkenyloxy, (2-4C)alkynyloxy, halogen X is SO2, CH2, C(O) or X is absent R4 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-6C)cycloalkyl, (3-6C)cycloalkenyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl, (2-6C)heterocycloalkyl(14C)alkyl, (6-1 OC)aryl, (6-10C)aryl(1-4C)alkyl, (1-9C)heteroaryl or (1-9C)heteroaryl(14C)alkyl. The compounds are useful for the treatment of fertility disorders.
EP1066304B1 Macrolide lhrh antagonists Disclosed are 3'-N-desmethyl-3'-N-susbstituted-6-O-methyl-11-deoxy-11, 12-cyclic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.
CN103040098A Lavender odor type snuff The invention belongs to the technical field of snuff products and relates to lavender odor type snuff made of a natural material and a preparation method of the snuff. The snuff comprises, by weight, 100-500 parts of green tea, 0.05-0.35 part of musk, 50-150 parts of blond magnolia flower, 10-90 parts of ophiopogon roots, 100-300 parts of mint leaves, 0.1-0.4 part of borneol, 0.03-0.10 part of asarum, 0.01-0.09 part of rhinoceros horn, 5-15 parts of notopterygium roots, 25-125 parts of tobacco leaves, 2-6 parts of agilawood, 2-6 parts of cloves, 5-25 parts of angelica roots, 2-6 parts of menthol, 50-150 parts of red wine and 5-10 parts of lavender. The snuff is smoked by the lavender and has the lavender odor. The snuff can produce refreshing effect to the mind, ventilate the nasal cavity and assist in smoking quitting.
EP0946557B1 A-1-adenosine receptor antagonists A compound useful as an A1 adenosine receptor antagonist has formula (I), wherein R1 is selected from the group consisting of C1-C8alkyl; R2 is of formula (II), wherein n is an integer ranging from 1 to 8; R5 is H or CH3(CH2)p, wherein p is an integer ranging from 1 to 7; and R6 is H; (CH2)mH; or (CH2)mOH, wherein m is an integer ranging from 1 to 8; R3 is selected from the group consisting of: (a), (b), (c) and (d), wherein q is an integer ranging from 1 to 8; D is selected from the group consisting of NH, S, and O; wherein R7 is selected from the group consisting of H, OH, NH2, R9COOH, wherein R9 is an alkylene or alkenylene group having 1 to 8 carbon atoms, and (CH2)tOH, wherein t is an integer ranging from 1 to 8; R11 is selected from the group consisting of -CH2COOH and -CH2-CONH(CH2)wNHZ, wherein w is an integer ranging from 1 to 2 and Z is selected from the group consisting of hydrogen and acetate; and R4 is of formula (III), wherein R8 is selected from the group consisting of H; OH; (CH2)fNH2 wherein f is selected from the group consisting of 0 and an integer ranging from 1 to 8; (CH2)sOH, wherein s is an integer ranging from 1 to 8; and R10COOH, wherein R10 is an alkylene or alkenylene group having 1 to 8 carbon atoms; and r is an integer ranging from 1 to 8.
CN102579430A Composition of meropenem and L-arginine The invention relates to a composition of antibiotics, in particular to a composition consisting of carbapenem antibiotics, i.e., meropenem and L-arginine. The composition contains the meropenem and the L-arginine, wherein the optimal weight ratio of the meropenem to the L-arginine is 2.2:1 (calculated on a dry and pure basis by a method according to Chinese Pharmacopoeia). The composition is difficult to demix after being vibrated, and the content uniformity is qualified; when the composition is added into 5 percent glucose or (and) 0.9 percent sodium chloride large-volume infusion for use, the stability of the solution is obviously improved compared with the stability of the composition of meropenem and sodium carbonate; and the composition is more stable and convenient and safer to use.
CN101628912B Anti-tumor compound containing triazole heterocyclic structure and application thereof The invention discloses a class of anti-tumor compounds containing a triazole heterocyclic structure and an application thereof, belonging to the technical field of medicinal chemistry. The compounds containing the triazole heterocyclic structure introduce quintuple 1,2,3-triazole ring in the form of side chains through the amino condensation, bromination, nitrine substitution, link reaction and other reactions on the basis of naphthalimide parent structure, select tetrazolium salt reduction to test 7721 hepatocellular in the experiment of inhibiting proliferation of tumor cells, and also select sulfonyl rhodamine B protein staining method to test MCF-7 breast cancer cells. The experiment results show that the anti-tumor compounds have wide anti-tumor activity and good inhibition effect on the normal growth of tumor cells derived from different tissues of liver cancer, breast cancer and the like.
US20090298937 Method for Inhibiting the Growth of Bacteria The present invention is directed to a method for inhibiting the growth of pathogenic bacteria in an infant formula comprising supplementing the infant formula with at least one diglyceride antimicrobial agent.
US20130035363 Thalidomide Analogs Thalidomide analogs that modulate tumor necrosis factor alpha (TNFα) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
USRE39762 e.g. 13-desmethoxy-18-hydroxyl-FK-520; compounds of the invention may be administered to achieve immunosuppression or to stimulate nerve growth and regeneration Polyketide compounds of the formula but not including FK-506, FK-520, 18-hydroxy-FK520 and 18-hydroxy-FK-506.
CN1602874A Sustained release preparation of propylthiouracil and its preparation method The invention discloses a propylthiouracil sustained-release preparation and its preparing method, and the weight percents of its components: propylthiouracil 10-70%, retarder 5-70% and medicinal auxiliary the rest, and it can be made into various forms, such as tablets, pilles, capsules, etc. Because it contains the retarder, it makes the releasing speed of propylthiouracil turn slow by the action of the retarder, and its release characteristic in pH-1.2 hydrochloric acid, water and pH-6.8 phosphate buffering liquor: accumulated release after 1h is 15%-40%, that after 4h 30%-80%, and that after 8h 70%-100%, thus producing slow, more stable blood drug concentration, assuring the concentration in curing window, beneficial to increase drug transportation to hypothyroid and simultaneously improve compliance of patients. It needs applying twice a day, 50-150 mg every time, thus reducing number of drug applying times and convenient to take.
CN101889987A Method for preparing novel cefixime tablets and cefixime capsules The invention provides a method for preparing novel cefixime tablets and cefixime capsules. In the method, cefixime, a solubilizer and water soluble auxiliary materials are micronized and then mixed with other auxiliary materials, and the obtained products are granulated by a dry method, so that the stability of cefixime tablets and cefixime capsules is improved, and the dissolution rate of cefixime is also raised. The cefixime can be quickly absorbed by a patient after the patient takes the cefixime tablets and cefixime capsules, the plasma peak time is shortened and the plasma concentration can be quickly stabilized at a higher level, so that the treating effect is improved.
US6852734 Indole wherein A is an oxygen atom or a nitrogen atom which nitrogen atom is optionally substituted with an alkyl group, and (i) R1 and R2 each stand for a hydrogen atom or an alkyl group, independently, or (ii) R1 and R2 as taken together form According to this invention, there is provided an indole derivative having the general formula (I) wherein A is an oxygen atom or a nitrogen atom which nitrogen atom is optionally substituted with an alkyl group, and (i) R1 and R2 each stand for a hydrogen atom or an alkyl group, independently, or (ii) R1 and R2 as taken together form a cycloalkyl group or an aromatic ring, or (iii) R1 and R2 as taken together form a heterocyclic ring, and R3 is a hydrogen atom, a (C1-C10)alkyl group or others, R4 is a substituted alkyl group and R5 is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group and so on, as novel compounds by a novel chemical synthetic process. The indole derivative of formula (I) exhibits a useful chymase inhibitory activity.
EP1616490A1 Composition comprising lutein, zinc and copper Composition containing lutein also contains zinc (Zn) and copper (Cu) compounds, preferably in the form of Zn gluconate and Cu(II) gluconate.
CN103304560A Thiazolinone derivatives comprising pyrazoline and thiophene (or furan) structures, and preparation method and application thereof The invention relates to thiazolinone derivatives comprising pyrazoline and thiophene (or furan) structures, and a preparation method and an application thereof. The derivatives are characterized in that the derivatives have a general formula presented as the following, wherein R is as the following, and X is S or O. Specifically, when R is as the following, X is S. The thiazolinone derivatives can be adopted as potential antimicrobial and antitumor medicines. The invention also discloses a preparation method thereof.
EP1865990B1 Method of treating type-2 diabetes The present invention is generally related to a method of treating, preventing, or reducing the risk of developing type-2 diabetes, and, more particularly, is related to a method of administering a transdermal hydroalcoholic gel composition to treat or prevent type-2 diabetes and a method of administering a transdermal hydroalcoholic gel composition to increase glycemic control in a subject in need thereof.
WO2006037848A1 Method and preparation for binding aldehydes in saliva The object of the invention is the use of compounds comprising one or more free sulphhydryl and amino groups for preparing a composition for locally binding aldehydes in saliva during smoking. The preferred compounds are cysteine and its derivatives. Also claimed are methods for decreasing the risk of smoking related cancers by using a composition of aldehyde binding substance(s), and a composition comprising aldehyde binding substance(s), characterized in that the composition is attached to or combined with a tobacco product, filter or holder.
CN101011527B Improved preparation of Juhong pill, its preparation method and quality inspection method The invention relates to a reddish orange capsule prepared from the following steps: (1) proportioning 15 kinds of medicinal materials, disintegrating dried orange peel into mesh fines, sieving, extracting the available compositions with dissolvent, making thick grease from the extract, (2) charging dried orange peel into the thick grease, mixing homogenously, drying into dried grease, and disintegrating the dried grease into mesh fines, (3) charging auxiliary materials and mixing homogeneously to obtain particles, (4) making capsules from the particles.
WO2013013504A1 Tigecycline derivative The invention belongs to the medicinal technical field, and in particular relates to a tigecycline derivative of general formula (I), a pharmaceutically acceptable salt, precursor drug, solvate or isomer thereof, wherein R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13, X and W are defined as in the description; the invention also relates to a preparation method of these compounds, a pharmaceutical composition containing these compounds and the use of these compounds in preparing medicines for the treatment and/or prevention of diseases with a sensitivity to tetracycline medicines.
EP2388255A1 Polysubstituted benzofurans and medicinal applications thereof The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or chemoprevention of cancer, aging related diseases or processes, diabetes and neurodegenerative diseases.
CN102716086A Carboxylated polyethylene glycol-polylactic acid segmented copolymer brucine nanoparticles and application thereof The invention, belonging to the field of medicinal preparation, specifically relates to carboxylated polyethylene glycol-polylactic acid segmented copolymer brucine nanoparticles and an application thereof. The nanoparticles are prepared by using brucine as an active component and using carboxylated polyethylene glycol and polylactic acid as the medicine excipients, wherein the brucine content in the nanoparticles is 4.2-4.6 %, and the entrapment efficiency is 67-82 %. In the application of the brucine nanoparticles of the invention in treating liver cancer, after peripheral intravenous administration, the carboxylated polyethylene glycol/polylactic acid segmented copolymer nano carrier can increase the brucine concentration in liver tumor issues to locally slowly release the medicine, prolong the action time to the tumor issues, raise the local medicine concentration, and reduce the general toxicity of brucine. The nanoparticles of the invention have the advantages of stable medicine concentration in the tumor issues and stable medicine release, good anticancer effect, safety and the like. The nanoparticles of the invention have good clinic application prospect.
WO2005021559A3 Oxazaborolidines as bacteria effectors The invention relates to a composition for modulation of at least one bacteria-related parameter comprising oxazaborolidine derivative compounds. The invention additionally relates to new oxazaborolidine derivative compounds. The invention further relates to a composition for decreasing bacterial growth, a composition for increasing the susceptibility of bacteria to the cytotoxic effects of other antibacterial agents, and a pharmaceutical composition comprising as an active ingredient an oxazaborolidine derivative compound. Methods for modulating at least one bacteria-related parameter, for preventing, decreasing or eliminating bacterial growth, and for making bacteria more susceptible to other antibacterial compounds are also described.
US20070244115 Amino-Halogen-Imidazopyridines as Proton Pump Inhibitors The invention relates to compounds of the formula (1) and to medicaments comprising these compounds.
CN102030805B Theasapogenol derivative with anti-tumour activity and preparing method and application thereof The present invention discloses a theasapogenol derivative with anti-tumour activity and preparing method and application thereof. The theasapogenol derivative with anti-tumour activity has a structure shown as formula I; and the preparing method comprises the following steps of: (1) reacting theasapogenol, which is the raw material, with trityl chloride in a pyridine solvent by using 4-dimethylamino pyridine as a catalyst, reacting the reaction product with benzyl bromide, and reacting the product thereof with formic acid to obtain alcohol terpenoid compound; (2) introducing in methylsulfonyl at C-28 bit based on the alcohol terpenoid compound; introducing in cyano at the C-28 bit with NaCN as a cyaniding reagent; and finally removing benzyl at palladium/carbon under hydrogen reduction condition, so as to obtain the theasapogenol derivative with anti-tumour activity shown as formula I. The theasapogenol derivative of the present invention has high anti-tumour activity; the preparing method and process are simple; and the theasapogenol derivative is convenient for industrial production.
WO2014065297A1 Silicon-containing compound aqueous solution and antibacterial/antiviral agent including said solution [Problem] To provide an antiviral/antibacterial agent comprising an aqueous solution and having excellent stability and odor-eliminating effects over time, the aqueous solution containing a dissolved silicon-containing compound having an antibacterial functional group. [Solution] An aqueous solution including a cyclodextrin or cyclodextrin derivative and a silicon-containing compound expressed by general formula (1) shown below (in the formula, R1 represents a hydrocarbon group having a carbon atomic number of 6 or greater; R2 and R3 represent the same or different lower hydrocarbon groups; R4 represents a divalent lower hydrocarbon group; R5, R6, and R7 represent the same or different lower alkyl groups or lower alkoxy groups; and X represents a halogen or organic carbonyloxy ion).
WO2008031771A3 3-azabicyclo [4. 1. 0] heptane derivatives for the treatment of depression The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof: formula (I), wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; such G may be substituted by (R2)p, which can be the same or different; R1 is hydrogen or C1-4alkyl; R2 is halogen, hydroxy, cyano,C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to R8; R5 is hydrogen or C1-4 alkyl; R6 is hydrogen or C1-4 alkyl; R7 is selected in the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to X, X1, X2 or X3; wherein X corresponds to: formula (a) X1 corresponds to: formula (b) X2 corresponds to: formula (c) X3 corresponds to: formula (d) R3 is hydrogen or C1-4 alkyl; or corresponds to X or X1; R4 is hydrogen or C1-4 alkyl; or corresponds to X or X1; R8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents selected from a group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R9 is C1-4alkyl; R10 is hydrogen, C1-4alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-3alkyl; R11 is haloC1-2alkyl; p is an integer from 0 to 5; n is 1 or 2. processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
CN100999494A Compound with action of anti-HIV and malignant tumour and its preparation process and use This invention relates to an anti-HIV and malignant tumor compounds and the preparation methods and application. The preparation method is: take quinolinic acid as raw materials, add the ether, 30% hydrogen peroxide, caustic soda and glacial acetic acid in turn; then under 150 to 255 deg heating and backstreaming for 1 to 2 hours; at last standing for 20 hours and separate out sediments to get these compounds. The present invention is improving on the basis previous studies of quinoline compounds which has anticancer and analgesic effect. And by animal experiments show that using this compound to treat animals which attacked by the current internationally recognized tumor virus strain ,after 70 days animals have survived in good shape and did not have any toxicological responses. This showed that the compounds has no side toxic effect, and has a clear anti-HIV and cancer role. In addition, the preparation method is simple and therefore suitable for large-scale industrial production.
CN102977221A Preparation method of coix seed polysaccharide and application of coix seed polysaccharide The invention relates to a preparation method of coix seed polysaccharide. The preparation method comprises the following steps of: crushing and screening coix seeds first, and carrying out degreasing, water bath extraction, centrifugation, enzymolysis, concentration, alcohol precipitation and vacuum freeze drying and precipitation to obtain crude coix seed polysaccharide; and dissolving the prepared crude coix seed polysaccharide to obtain a crude coix seed polysaccharide solution, carrying out deproteinization, decoloration, dialysis and ion exchange chromatography on the crude coix seed polysaccharide solution to obtain purified coix seed polysaccharide, and then carrying out vacuum freeze drying to obtain white powder, namely the coix seed polysaccharide. According to the preparation method disclosed by the invention, the crude coix seed polysaccharide is extracted by using a water extraction and alcohol precipitation method, the crude coix seed polysaccharide is subjected to deproteinization, decoloration, dialysis and ion exchange chromatography to obtain the purified coix seed polysaccharide, and then, the purified coix seed polysaccharide is subjected to vacuum freeze drying to obtain the white powder, namely the coix seed polysaccharide; and therefore, the preparation method is simple and the coix seed polysaccharide is high in yield.
US20110257180 Novel Polymorphic Forms of 6-(1-methyl-1H-pyrazol-4-yl)-2--2H-pyridazin-3-one Dihydrogenphosphate and Processes of Manufacturing thereof The present invention relates to 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate, its solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
EP1751094A2 Beta-peptides β-peptide regions of polypeptides can serve as structural mimics of α-helices in wild type proteins. Because α-helices of one protein often bind to a target protein in a biological pathway, a polypeptide that contains a helical β-peptide region can be used to disrupt this type of protein-protein binding. As a result, polypeptides that contain a helical ß-peptide region can be used to treat conditions involving this type of protein protein binding, such as viral infections and cell proliferation.
US20070111956 Remedy for sarcoidosis and method of treating the same The present invention provides a remedy for sarcoidosis, one of systemic granulomatous diseases, and a method for treating sarcoidosis. A remedy for sarcoidosis containing a Propionibacterium acnes-targeting antibiotic such as minocycline hydrochloride and clindamycin as an active component is prepared. Further, sarcoidosis is treated by administering this remedy for sarcoidosis to sarcoidosis patients.
WO2014130810A1 C-3 alkyl and alkenyl modified betulinic acid derivatives useful in the treatment of hiv Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, alkyl and alkenyl C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: a compound of Formula I; a compound of Formula II; a compound of Formula III: and a compound of Formula IV. These compounds are useful for the treatment of HIV and AIDS.
WO2008016700A2 N-oxide compounds for therapeutics uses Compounds of formula (I) and a method of treating a patient suffering from certain inflammatory disorders, demyelinating disorders, FLT3-mediated disorders, CSF-1R-mediated disorders, cancers and leukemias, comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
US8354415 Thienopyrimidine compounds and compositions Compounds of formula (I) are A2B wherein R1 and R2 are independently selected from hydrogen, or optionally substituted CrC6 alkyl, C1-C6alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-(C1-C6)-alkyl; or R−1 and R2 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R3 and R4 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-C1-C6)-alkyl; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R5 and R6 are independently selected from hydrogen, C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl, —NHR7—N(—R8)—R9, —NH—(C═O)—R10, —(C═O)—NH—R11, —(C═O)—O—R12, or halo; and R7, R8, R9, R10, R−11, and R12 are independently selected from C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl and heteroaryl.
WO2006069533A1 Desmosdumotins, their manufactures and use as antitumor and anti-aids agent The invention discloses a method for preparing desmosdumotin C, the series of desmosdumotin C derivatives and their manufactures, and the total synthesis of desmosdumotin B. The invention also discloses applications of the derivatives and medicinal compositions containing them in manufacturing medicines for treating tumor or AIDS.
US20110268771 Chewable gelled emulsions An oral pharmaceutical composition in unit dose form, each unit dose comprising a lipophilic drug substance within a unitary carrier body, said body comprising a soft, chewable, gelled oil-in-water emulsion.
WO2011058109A1 Fused bicyclic pyrrole and imidazole derivatives as kinase inhibitors A series of substituted pyrrolo[2,1-ƒ][1,2,4]triazine and imidazo[2,1-ƒ]-[1,2,4]triazine derivatives, and fused pyridazine analogues thereof, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions (Formula (I)).
CA2410745C Process for converting the carbonyl function in position 4" of the cladinose unit of an aza-macrolide into an amine derivative The invention relates to a process for preparing compound of general formula I (see formula I) by reductive amination of the corresponding (4")-carbonyl derivative, characterized in that it comprises:- placing the said (4")-carbonyl derivative in contact with at least one nitrogenous reagent and a Lewis acid under conditions that are favourable for converting the 4" carbonyl function, - reducing the resulting mixture using a reducing agent, and - optionally deprotecting the hydroxyl function in position 2', to give the expected compound of general formula I.
CN101269217A Compound digestive enzyme locating release capsule The invention relates to a compound digestive enzyme positioning and releasing capsule prescription and a preparation process thereof. The capsule consists of three micro-tablets which respectively release medicine in the upside of the stomach, in the antrum of the stomach, and in the intestines thereof; during preparation, the main medicine and the auxiliary medicine contained in the tablets are pressed into three different tablets, the respective tablets are covered with film coatings released under different pH conditions so as to achieve the purpose of releasing in different sites. Compared with the prior similar products, the compound digestive enzyme preparation of the invention has better positioning and releasing effect, as well as more comprehensive and higher enzyme vigor.
US7300663 Adhesion and sealing of tissue with compositions containing polyfunctional crosslinking agents and protein polymers Proteinaceous polymers having repetitive units from naturally occurring structural proteins are employed as backbones for functionalities for crosslinking to provide strongly adherent tissue adhesives and sealants. Particularly, block copolymers of elastin and fibroin are employed having lysine substitutions in spaced apart units, where the amino group can be crosslinked using difunctional crosslinking agents.
WO2009133647A1 Polymerized cyclic nitroxide radical compound, and use thereof Disclosed are: a method for covalently binding a cyclic nitroxide radical compound to a hydrophobic block in a specific hydrophilic-hydrophobic block copolymer; a polymerized cyclic nitroxide radical compound which is produced through the covalent binding by the method; and use of the compound in the medical field or the like. The compound exhibits long-term stability in vivo under a reductive environment.
CN103086994A Salts of isoxazole derivatives The invention relates to applications of fumarates of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholine-4-yl-methyl-phenyl)-isoxazole-3-ethylformamide and derivatives thereof, or pharmaceutically acceptable solvates in the preparation of medicines for treating cancers.
CN1879815A Compound decoction with astragalus root for birds and method for preparing same The invention discloses a fowl use beverage and process for preparation, wherein the beverage is prepared from astragalus root 1-3 parts, plaster stone 1-3 parts, licorice root 1-3 parts, and cogongrass rhizome 1-3 parts through the steps of chopping, merging, homogenizing, grilling with water, filtering and concentrating.
CN102850283A Triazolyl-containing amino-dithio formic ether compound as well as preparation method and application of compound The invention discloses a triazolyl-containing amino-dithio formic ether compound as well as a preparation method and application of the compound which is taken as a new antineoplastic medicament lead compound, belonging to the field of pharmaceutical chemistry. According to the invention, 1, 2, 3-triazole active fragment is introduced into the structure of amino-dithio formic ether by click chemistry, thus the preparation method is simple, efficient and environment-friendly. The triazolyl-containing amino-dithio formic ether compound has the structure general formula shown in the specification, and has excellent antineoplastic activity for multiple tumour cells, can be used as a candidate or lead compound for the further development to be applied to the preparation of the antineoplastic medicaments.
EP1565453A1 2- (4-benzyl)-1-piperidinyl)methyl]benzimidazole-5-ol derivatives as nr2b receptor antagonists 2-[(4-Benzyl)-1-piperidinyl)-methyl]benzimidazole-5-ol derivatives are NMDA NR2B receptor antagonists useful in the treatment of pain and other NMDA mediated diseases.
US20080200504 non-peptide NK-3 receptor ligands; anxiety, depression, schizophrenia, obesity; 2-Phenyl-quinoline-4-carboxylic acid (1-pyridin-4-yl-propyl) amide; reacting the 2-phenyl-quinolinyl-4-carbonyl chloride with a pyridylalkylamine to form the amide Compounds of Formula (I) wherein R1, A, R2, R3, R4, R5,n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
EP1280514B1 Evaporative coolant comprising hydrofluorocarbons Evaporative coolants suitable for use as cold spray topical anesthetics containing hydrofluorocarbons and/or hydrochlorofluorocarbons, preferably 1,1,1,3,3-pentafluoropropane, either alone or in combination with other hydrofluorocarbon and/or hydrochlorofluorocarbon components. The invention includes a system for cooling skin using the coolant and a device for spraying the coolant, as well as a method of cooling or topically anesthetizing the skin comprising spraying such evaporative coolants thereon.
DE102009041048A1 Topically applicable pharmaceutical composition, useful for treating skin diseases e.g. actinic keratosis, comprises a frankincense extract or a frankincense active material and hyaluronic acid or its derivatives Topically applicable pharmaceutical composition for the skin comprises: a frankincense extract or a frankincense active material; and hyaluronic acid or its derivatives. - ACTIVITY : Keratolytic; Dermatological; Antiinflammatory; Gastrointestinal-Gen. No biological data given. - MECHANISM OF ACTION : None given.
WO2014085909A1 Methods and kits for monitoring response to radiation therapies in cancer A method of evaluating a cancer cell sample, the method comprising: a. obtaining a cancer cell sample, optionally a breast cancer cell sample or an ovarian cancer cell sample, after the cancer cells have been exposed to a radiation dose; b. assaying the cancer cell sample to obtain a RNA integrity value and/or a RNA concentration of the cancer cell sample.
US20080044452 Drug delivery system for treatment of transitional cell carcinoma A system for treating tissue carcinomas and benign inflammatory conditions of the urinary tract includes a flowable medium containing a bioactive agent and a thermogelling aqueous polymer solution. The thermogelling aqueous polymer solution maintains the bioactive agent within the urinary tract for a therapeutically optimal period of time. One embodiment includes delivering a bioactive agent in a flowable medium through an orifice into a body cavity, contacting the tissue to be treated with the bioactive agent, and filling the orifice of the body cavity with a thermogelling aqueous polymer solution. The polymer solution maintains the bioactive agent in contact with the tissue to be treated for a therapeutically optimal period of time.
US20050048043 Methods for in vivo gene transfer into pancreatic and biliary epithelial cells The present invention relates to methods for selective somatic gene transfer into a patient's pancreatic or biliary epithelial cells. The methods of this invention comprise introducing the gene to be transferred, associated with an appropriate transfer vehicle, into the ductal system of either the pancreas or liver. More specifically, the invention relates to using these techniques to treat genetic diseases, such as cystic fibrosis, which are characterized by genetic defects in those epithelial cells.
WO2014020350A1 Par2 receptor antagonists Compounds of formula (I) or pharmaceutically acceptable salts, solvates or hydrates thereof wherein P, Q, X, Y, R1, R2, R3, R10, R11, and R12 are as defined in the claims, and the use those compounds in medicine.
CA2685321A1 Solubilized delivery system for topical anesthetics A nano particle drug delivery system comprised of micelles coated with lipid molecules for the non-invasive deployment and absorption of active anesthetic compounds through the stratum corneum and throughout the skin and sub cutaneous tissue without any cutaneous toxicity.
EP1301194B1 Essential oil combination and therapeutic uses thereof The invention concerns the combination of at least two essential oils selected among Helichrysum Italicum ssp Serotinum, Ledum Groenlandicum and Ravensara Aromatica essential oils, for simultaneous, separate or prolonged use, and the therapeutic uses thereof.
DE102006034320A1 Antioxidant, useful for preparation of e.g. coloring agent, vesicle, dermocosmetic, pharmaceuticals and nutrient- or feedstuff, comprises at least an isorenieratene compound Antioxidant comprises at least an isorenieratene compound (I). Antioxidant comprises at least an isorenieratene compound of formula (I). R1>H or easily splittable protecting group; and R2>-R4>1-3C-alkyl. Independent claims are included for: (1) mixture (M1) comprising at least (I) and 3,3'-dihydroxyisorenieratene-1-quinone (II) and/or 3,3'-dihydroxy-2,2',4,4'-tetra-tert-butylisorenieratene-1-quinone (III); (2) mixture (M2) comprising 3,3'-dihydroxy-2,2',4,4'-tetra-tert-butyl isorenieratene (IV) and at least (I) or (M1); (3) preparation (V) comprising (I), (II), (III) and/or (IV); (4) dermocosmetic, pharmaceutical and nutrient or feedstuff comprising (V); (5) solid material and/or liquid comprising (V); (6) coloring agent (A) comprising (II) or (III) or (IV) or (M1) or (M2); (7) coloring agent (B) comprising (V) in the form of H- or J-aggregate; (8) dermocosmetic, pharmaceutical, and nutrient or feedstuff comprising (A) or (B); (9) solid or liquid material comprising (A) or (B); (10) vesicle comprising (V); (11) dermocosmetic, pharmaceutical and nutrient- or feed stuff comprising the vesicle; (12) solid or liquid material comprising the vesicle; (13) carotenoid-formulation comprising (V); (14) preparation (VI)comprising the carotenoid formulation or (V); (15) dermocosmetic, pharmaceutical and nutrient or feedstuff comprising the carotenoids formulation or (V); (16) gelatin capsule comprising the carotenoids-formulation or (V); and (17) preparation of antioxidant, (M1) or (M2), (V), (A), vesicle, carotenoid-formulation, dermocosmetic, pharmaceutical, nutrient- or feedstuff, gelatin capsule or solid or liquid material comprising mixing (V), antioxidant, (M1) or (M2), (VI), (A), vesicle or carotenoid formulation. [Image]
CN102716076A Ambroxol hydrochloride medicine combination for injection The invention discloses an ambroxol hydrochloride medicine combination for injection. The ambroxol hydrochloride injection is composed of ambroxol hydrochloride, sodium chloride, glacial acetic acid and sodium acetate, wherein each ambroxol hydrochloride injection is composed of 15-30mg of ambroxol hydrochloride, 18-36mg of sodium chloride, 10-20mg of glacial acetic acid and 2.52-5.1g of sodium acetate. The preparing method includes: taking 90% of water for injection as the prescription amount; adding the glacial acetic acid and the sodium acetate as the prescription amount for stirring to dissolve the glacial acetic acid and the sodium acetate at the temperature of 55-65 DEG C; adding the ambroxol hydrochloride as the prescription amount, stirring to dissolve the ambroxol hydrochloride, adding the sodium chloride as the prescription amount in the solution, and stirring to totally dissolve the sodium chloride; measuring the initial pH value, regulating the pH value to be within the range of 3.5-4.5 with 10% glacial acetic acid solution; adding 0.05% of medical carbon in the solution, stirring and standing for 30 minutes; performing suction filtration, replenishing injection water to full amount, and evenly mixing; performing fine filtering; filling; sterilizing for 15 minutes under hot pressure at the temperature of 121 DEG C; performing lamp inspection; warehousing; and obtaining the ambroxol hydrochloride injection. The ambroxol hydrochloride medicine combination is good in photo-stability and stability, improves product yield, reduces cost, achieves industrialization, can be better applied to clinical medicine and has obvious advantages.
US7201922 Codried granules of lactose and starch with an active substance The subject of the invention is an orodispersible solid pharmaceutical form characterized in that it comprises: granules consisting of lactose and starch which have been codried; at least one active substance. The subject of the invention is also the use of codried granules consisting of lactose and starch for the preparation of orodispersible solid pharmaceutical forms.
CN103623052A Novel method for preparing danxiang (Chinese character) rhinitis tablet The invention provides a novel method for preparing a danxiang (Chinese character) rhinitis tablet. Essential oil is extracted from pogostemon cablin and centipeda minima in the traditional prescription by virtue of a steam distillation method, and the residue is subjected to ethanol extraction. By adopting the novel technology, alcohol-soluble active ingredients are reserved, extracted volatile active ingredients are increased, loss of the effective ingredients is reduced, and the curative effect of the product is improved.
EP2419104A2 5-ht4 receptor agonist compounds for treatment of cognitive disorders The invention relates to the use of specific 5-HT4 receptor agonist compounds for the treatment of cognitive disorders, in particular, to the use of these compounds in combination with other agents, specifically acetylcholinesterase inhibitors, for the treatment of Alzheimer's disease and other cognitive disorders.
US8415326 Pharmaceutical composition comprising chito-oligomers Compositions are provided comprising chito-oligomers obtainable from chitin, comprising oligomers of N-acetyl glucosamine (NAG) and glucosamine, wherein at least 50% of the oligomers have a chain length of about 2-50, and the degree of deacetylation of the oligomers is in the range of about 0-70%, preferably about 30-50%. The compositions are highly useful as pharmaceutical compositions for treatment of joint disorders such as rheumatoid arthritis and osteoarthritis. Also provided are methods for treatment of joint disorders and treatment against inflammatory activity.
US20090022655 boron neutron capture therapy, attaching antibody (IgG) cell-targeting species to BN nanostructures to form composite, administering to target tumors, activating boron in composite; indirect source of radiation therapy, delivery vehicles for radio- and chemo-therapeutic materials, imaging agents The present invention provides a novel approach to cancer therapy and diagnostics that utilizes nanotubes and other similar nanostructures as both an indirect source of radiation therapy (BNCT), and as delivery vehicles for other types of radio- and chemo-therapeutic materials, as well as imaging agents for diagnostic purposes.
CN101417969A Cinnamoyl pyrrolidine derivates and preparation method and use thereof The invention discloses a cinnamoyl pyrrolidine derivative and a preparation method and application thereof. The cinnamoyl pyrrolidine derivative is a compound of a formula (I), wherein R1 is hydrogen or C1 to C4 of alkanes; R2 is a cyano group, an acidic group, an ester group, an amino group or a substituted amino group, and the substituted group is straight chain alkanes of C1 to C4 or naphthenic bases of C3 to C6. The invention also discloses the preparation method for the compound and the application thereof in preparation of drugs for treating or preventing non- insulin-dependent diabetes, obesity, arthritis or other glucose tolerance abnormality diseases.
US20090274693 Method of Treating Cancer using a cMet and AXL Inhibitor and an ErbB Inhibitor The present invention relates to a method of treating cancer in a patient comprising administering to the patient therapeutically effective amounts of: a) a compound of formula A: or a pharmaceutically acceptable salt thereof, wherein R1-R4, p, and q are as defined; and (b) an erbB inhibitor that inhibits erbB-1 or erbB-2 or erbB-3 receptor or a combination thereof. The method of the present invention addresses a need in the art with the discovery of a combination therapy that shows evidence of being a more effective therapy than previously disclosed therapies.
US20100222388 Enhanced Migraine Treatments Based on Ghrelin Mimetics The present invention relates to method of enhancing the absorption of migraine medications and thereby treating migraines by co-administering to a subject in need thereof an effective amount of a ghrelin mimetic or pharmaceutically acceptable salt, hydrate or solvate thereof and at least one migraine medication selected from a serotonin 5-HT1B/1D receptor agonist, a tryptamine derivative, an ergoline derivative, a non-steroidal anti-inflammatory drug, or an analgesic, or any combination thereof.
CA2422531C Topical analgesic compositions containing aliphatic polyamines and methods of using same A method for producing local analgesia in a subject having a site of local discomfort. A composition to be administered includes an aliphatic polyamine. The polyamine can be an alkylamine. Particular amines include putrescine, spermine, spermidine and cadaverine. The composition can also include urea and/or lidocaine.
CN103237547A Crystalline naloxol-eg conjugate Naloxol-polyethlyene glycol conjugates of the formula are provided in oxalate or phosphate salt forms including crystalline forms. Methods of preparing the salt forms and pharmaceutical compositions comprising the salt forms are also provided.
CN102584767A Application of 4'-methoxy-7-hydroxy isoflavone in preparation of anti-tumor drugs and preparation method of 4'-methoxy-7-hydroxy isoflavone The invention relates to a preparation method of 4'-methoxy-7-hydroxy isoflavone compound for inducing expression of a nuclear receptor Nur77, and an application of the 4'-methoxy-7-hydroxy isoflavone. According to the 4'-methoxy-7-hydroxy isoflavone compound, the expression of the nuclear receptor Nur77 can be induced, so that the 4'-methoxy-7-hydroxy isoflavone can serve as an inducer to be applied to the preparation of drugs for preventing and treating cancers, tumors and the like.
EP1492548A1 Composition for the topical treatment of vulvovaginitis and mycoses Composition for the treatment of vulvovaginitis and other cutaneous mycoses, comprising bergamot and boric acid in appropriate percentages. The bergamot-boric acid composition has a synergetic effect because it allows to lower the amount of boric acid (which is toxic at high percentage ratios) without reducing the efficacy of the active principles (bergamot and boric acid). The invention further discloses administration means for the treatment of these kinds of mycoses, which are not limited to pessaries (treatment of vulvovaginitis), and further, it discloses some additives of the compound which are included in said administration means.
US20120252782 Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
US7799770 For use in female birth control, for therapy of hormone-dependent gynecological disorders and for hormone replacement therapy The invention relates to novel solid body forms of mesoprogestin 11β-[4E-(hydroxyiminomethyl)-phenyl]-17α-methoxymethyl-17β-methoxy-estra-4,9-dien-3-one (oxime J 867), particularly a highly pure and stable amorphous or highly crystalline form (ansolvate/anhydrate) of compound J 867. The invention also relates to methods for producing said novel solid body forms and to the use thereof in pharmaceutical compositions. The novel solid body forms are characterized by exhibiting a high degree of stability. The solid body forms of oxime J 867 can, in particular, be used in the area of fertility control and in hormone replacement therapy.
CN101921816A Preparation method and use of xanthone derivative The invention discloses a preparation method and use of a xanthone derivative. In preparation, a marine endophytic fungus strain is cultured in a stain culture medium first and then subjected to fermentation culture in a fermentation culture medium, liquid generated by the fermentation is filtered to remove fungi, and the obtained fermentation liquor is extracted by an organic solvent; and the obtained extract solution is concentrated, the concentrate is separated by column chromatography or thin-layer chromatography, and the obtained eluent is concentrated to form yellowish crystals which are the xanthone derivative. The xanthone derivative of the invention has high inhibiting activity for human nasopharyngeal carcinoma KB and human nasopharyngeal carcinoma medicament resistant stain KBV200 tumor cells and can be used as antitumor medicaments. The method has the advantages that: the raw materials can be used for large-scale production; and the application prospect is promising.
WO2011107494A1 Novel aromatic glycoside derivatives, medicaments containing said compounds, and the use thereof The invention relates to aromatic glycoside derivatives of the formula (I), in which the groups have the given meanings, to the physiologically acceptable salts thereof, and to methods for the production thereof. The compounds are suitable as antidiabetics, for example.
US20130210758 Formulation and method to induce a deep state of relaxation A relaxation formulation structured to induce a deep state of relaxation in a person comprises amounts of tryptophan, melatonin, vitamin B3, and vitamin B6. Another relaxation formulation also includes an amount of tyrosine, and yet another formulation includes an amount of vitamin B12. At least one embodiment of a relaxation formula comprises a physiologically effective amount of gamma-aminobutyric acid (“GABA”). A delivery system is provided to facilitate administration of the relaxation formulation to a person. The delivery system may include an edible high carbohydrate matrix, such as a chocolate brownie. Alternatively, the delivery system may comprise an inert vaporizable compound to allow the components of the relaxation formulation to be inhaled directly into the lungs of a person. Other delivery systems include an aqueous sublingual spray and a beverage.
US20100061932 Peptides useful as cell-penetrating peptides The present invention is related to a peptide having an amino acid sequence comprising at least 8 consecutive amino acids of the human lactoferrin protein or of the bovine lactoferrin protein, whereby the peptide is suitable to act as a cell-penetrating peptide.
EP1530473A2 Regulation of erythrocyte apoptosis The invention relates to the use of a substance for detecting cation channels and to the use of an active ingredient for influencing cation channels for the prevention or treatment of diseases associated with a defective regulation of apoptosis.
US6924282 5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydrox y-1,6-naphthyridine-7-carboxamide; preventing or treating hiv or aids A sodium salt of Compound A is disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for preventing or treating HIV infection, for delaying the onset of AIDS, and for treating AIDS.
US20120108633 Injectable composition containing hydroxychloroquine for local administration for treating hemorrhoids The present invention relates to an injectable composition for local administration for treating hemorrhoids, which contains hydroxychloroquine. Specifically, the composition contains a solution of hydroxychloroquine in physiological saline for injection, together with a local anesthetic and an antioxidant.
US7205411 for treatment of neuropathic pain The invention relates to novel aminopyridine derivatives of formula (I) wherein R1 is methyl an R4 and amino group —NR6R7 and R5 forms an arylalkynyl- or heteroarylalkynyl-group. The compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors
US8008333 Inducing ovulation; increasing response to follicle stimulating hormone The use of an aromatase inhibitor (AI) in the preparation of a medicament for use in inducing ovulation in a female suffering from anovulatory infertility which comprises administering to said female a single dose of the at least one aromatase inhibitor. The use of an aromatase inhibitor (AI) for the preparation of a medicament comprising a single dose of at least one aromatase inhibitor (AI) for administration to an ovulating female suffering from unexplained infertility or other types of ovulatory infertility early in one or more menstrual cycles. Such a medicament may also be administered to an anovulatory female in combination with a plurality of daily doses of follicle stimulating hormone (FSH) whereby the dosage levels of FSH may be reduced. The use of AI in the preparation of a medicament for administration to a female who is a poor responder to FSH, which comprises a combination of a single dose of AI with a plurality of daily doses of FSH is also disclosed. The related pharmaceutical preparations and packages are also described.
CN101851170A Chlocibutamine type II crystals The invention relates to chlocibutamine type II crystals. Positions of peaks in the characteristic spectrum shown in an X-ray powder diffraction pattern are roughly 7.5, 7.8, 13.4, 14.9, 15.5, 16.7, 18.7, 20.2, 21.1, 22.8, 23.2, 24.8, 26.0, 27.1 and 30.2 degrees 2 theta, and corresponding relative strengths are 19, 17, 30, 39, 100, 16, 52, 12, 38, 27, 16, 25, 21, 30 and 45 respectively. The invention also relates to a method for preparing the chlocibutamine type II crystals and compounds of the chlocibutamine type II crystals.
CN102020546A PTP1B inhibitor and preparation and application in preparing drug for treating type 2 diabetes mellitus thereof The invention relates to a chemical total synthesis method for a novel PTP1B inhibitor and the application in drugs for treating type 2 diabetes mellitus. The chemical structural formula of the PTP1B inhibitor is as follows, wherein each carbon at 2, 2', 3, 3', 6, and 6' position of a phenyl ring is connected with a group of bromine atom; each carbon at 4, 4', 5, 5' position is connected with a methoxyl; the chemical name in English is bis-(2,3,6-tribromo-4,5-dimethoxy-phenyl)-methanone. The compound enhances the sensitivity of insulin receptors by inhibiting the activity of protein tyrosine phosphatase 1B, and has good therapeutic effects on insulin resistant type 2 diabetes mellitus.
EP2404596A1 Kit for Cancer Treatment and Pharmaceutical Composition for Cancer Treatment To provide a kit for cancer treatment and a pharmaceutical composition for cancer treatment that can inhibit the growth of tumors and cancers in mammals more than ever. The kit for cancer treatment includes a combination of two different drugs in a kit formulation. The first drug contains a synthetic retinoid or a pharmaceutically acceptable organic or inorganic acid addition salt thereof, and the second drug contains a chemotherapeutic agent for cancer treatment. A synthetic retinoid that can be suitably used is a benzoic acid derivative represented by the following formula (I): or a pharmaceutically acceptable organic or inorganic acid addition salt thereof.
WO2013116228A1 Compounds and methods for inhibition of ap endonuclease-1/ redox factor-1 (hape1) activity A method for treating a neoplasm in a subject, comprising co-administering to the subject a therapeutically effective amount of an anticancer agent and a substituted 6,7-methylenedioxy-4-amino-quinoline, or a pharmaceutically acceptable salt or ester thereof.
US7507765 Mevalonic acid derivatives; antitumor/anticancer agents This invention provides compounds having excellent antitumor activity, which are represented by the following formulae in which R1, R2, R3, m, n and R4 have the significations as given in the specification.
WO2010072734A2 Targeting prodrugs and compositions for the treatment of gastrointestinal diseases Provided herein are compounds of formula (I) as well as compounds of formula (I) which are prodrugs in which the (R7)a-phenyl-S(O)2NH group represents a sulphonamide-bond compound, compositions and methods for preventing or treating gastrointestinal diseases such as inflammatory bowel disease and colorectal cancer, wherein the method comprises delivering an effective amount of a COX-2 or a similar sulphonamide inhibitor as a prodrug or a derivative thereof to the colon, wherein the COX-2 or similar inhibitor is released in vivo.
WO2010105096A3 Modulation of human cytomegalovirus replication by micro-rna 132 (mir132), micro-rna 145 (mir145) and micro-rna 212 (mir212) The present invention related to miR145, miR132, miR212, and the genes or gene products regulated by these miRNAs. miR145 is downregulated in cells infected with HCMV. This downregulation modulates expression of miR145 target genes, including IRS-I. Transfection of cells with a miR145 agent, such as a miR145 mimetic, reduces HCMV replication and protein expression. miR132 and miR212 are upregulated in cells infected with HCMV. This upregulation modulates expression of miR132 and miR212 target genes, including MeCP2 and RICS. Transfection of cells with a miR132 and/or a miR212 antagonist reduces HCMV replication and protein expression. Accordingly, the invention provides methods of attenuating HCMV replication by modulating, for example, miR145, miR132, and/or miR212, and targets thereof. Also provided are methods of detecting an HCMV infection, and compositions and kits useful for attenuating HCMV replication.
US7265127 Imidazo[1,2-a]pyridine derivatives, especially N-(2-(8-(3-aminocarbonyl-2-pyridyloxy)imidazo[1,2-a]pyrid-3-yl)-1,1-dimethylethyl)-3-(o-isoxazol-3-ylphenoxy)-2-hydroxypropylamine; treating type-2 diabetes and obesity The present invention relates to 2-imidazo[1,2-a]pyridine group containing β3 adrenergic receptor agonists or pharmaceutical salts thereof.
CN1559390A Oral disintegration tablets contg. p-acetaminophenol, and prepn. method therefor An oral disintegrating tablet of paracetamol is prepared from paracetamol, water-soluble filler, disintegrant, lubricant, and wetting agent or adhesive.
US20090005325 Ketolide Derivatives as Antibacterial Agents Provided herein are ketolide derivatives, which can be used as antibacterial agents. Compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus, Enterobactericeae, Propionibacterium acnes or any combination thereof. Also provided are processes for preparation of compounds described herein, pharmaceutical compositions thereof, and methods of treating bacterial infections.
CN1927208A Preparing technique for stomatocace film The invention relates to a film agent for treating ulcerative stomatitis, which comprises acetic chlorhexidine, prednisone hydrochloride, desicaine hydrochloride, glycerin, polyvinyl alcohol, starch, cellulose glycollic ether, edible lemon yellow, polyester film and distilled water.
US20120122949 Ultra-high strength injectable hydrogel and process for producing the same [Problem] The present invention is intended to provide high-strength hydrogels and method for fabricating the same. The present invention is intended to provide the method for fabricating the hydrogels with different decomposition rates. [Solution to Problem] The present invention is based on a knowledge that high-strength hydrogels can be fabricated by controlling pH of solution, ionic strength in the solution, and buffer concentration in the solution. In addition, the present invention is based on a knowledge that the high-strength hydrogels which have homogeneous macromolecular network structure can be fabricated by polymerizing four-branching compounds after having dispersed the four-branching compounds homogeneously.
WO2010095106A1 Solid forms of ( 2r) -2- { ( is ) -6, 7 -dimethoxy- 1- [2- (4-triflu0r0methyl-phenyl) -ethyl] -3, 4-dihydr0-1h -isoquinolin-2-yl} -n-methyl-2-phenyl-acetamide hydrochloride The invention relates to hydrated crystalline forms of (2R)-2-{(1 S)-6,7-dimethoxy-1 - [2-(4-thfluoromethyl-phenyl)-ethyl]-3,4-dihydro-1 H-isoquinolin-2-yl}-Λ/-methyl-2- phenyl-acetamide hydrochloride, to the amorphous form of this compound, and to further crystalline forms of this compound, to processes for the preparation thereof, pharmaceutical compositions containing said crystalline forms or said amorphous form, and their use as orexin receptor antagonists.
WO2010080756A2 Harmine derivatives for reducing body weight The present invention provides a method of reducing body weight in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of obesity and disorders related to obesity and higher than recommended percentage body fat, such as type II diabetes.
CA2729597A1 Method of treating traumatic brain injury This invention provides for methods of treating a subject suffering from central nervous system injury, including traumatic brain injury, comprising administering to the subject an amount of a perf luorocarbon. This invention also provides for use of a perf luorocarbon in the manufacture of a medicament for treating a subject suffering from central nervous system injury including traumatic brain injury. This invention further provides for a pharmaceutical composition comprising a perf luorocarbon for use in treating a subject suffering from central nervous system injury, including traumatic brain injury.
WO2008106772A1 Phospholipid compositions with improved bioavailability and methods for their use The invention provides pharmaceutical compositions for oral administration comprising a phospholipid having an enteric coating, in an effective amount for treating or preventing dyslipidemia or atherosclerosis. Methods of using these compositions are also provided. Also provided is a method wherein the above -described phospholipid is administered in combination with an antacid agent or proton pump inhibitor.
CN103156864A Application of triptolide in medicine used for inhibiting rheumatoid arthritis (RA) synovial angiogenesis The invention provides application of triptolide in a medicine used for inhibiting RA synovial angiogenesis. The triptolide provided by the invention can be applied in the medicine used for inhibiting RA synovial angiogenesis, so novel application of Tripterygium wilfordii Hook. f is opened up, and a novel option is provided for the medicine used for inhibiting RA synovial angiogenesis.
WO2006072792A3 Compounds which bind to the active site of protein kinase enzymes One or more compounds that are inhibitors of a serine/ threonine kinase, more particularly Rho kinase (ROK, ROCK) can be used in the manufacture of a medicament for treatment or prophylaxis of a condition selected from: an ocular condition including age related macular degeneration, lacrimal gland disease or diabetic retinopathy, or suppression of neurite growth and hence a condition requiring nerve cell extension and connectivity, neuronal regeneration, inducing new axonal growth and promotion of axonal (re)wiring, repairing damage to neurons in the CNS caused by trauma (eg stroke, traumatic brain injury etc.) or neurodegeneration (eg Alzheimer's, Parkinson's etc), repair and recovery from and treatment of disorders such as spinal cord injury and in reducing the subsequent effects thereof, or pain caused by nerve cell damage such as following trauma or amputation for example in the treatment of neuropathic pain. The compounds are selected from the specific group of compounds that comprises or consists of compounds of formula (I) or (II) wherein R1, R2, R3, R4, R5 and R6 are defined herein.
CN103479572A 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride microemulsion and preparation method thereof The invention discloses a 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride microemulsion and a preparation method thereof. A formula of the 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride microemulsion contains 5-30mass% of 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride, 10-30mass% of an oil phase, 5-20mass% of a surfactant, 10-30mass% of a cosurfactant, and the balance water phase. The preparation method comprises the following steps: uniformly mixing the 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride with the surfactant according to the formula, uniformly mixing with the cosurfactant, uniformly mixing with the oil phase, and uniformly mixing with the water phase. The 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride microemulsion has a good bioavailability.
EP1071412B1 Use of quinolinate for treating gastrointestinal disorders 'Black holes' in the genomes of bacterial pathogens represent deletions of 'anti-virulence' genes, i.e. genes that are detrimental to a pathogenic lifestyle. Identification of the missing genetic loci in the 'black hole' identifies genes that are incompatible with the bacteria's pathogenicity. These genes, their gene products, and compounds generated by the enzymatic action of these gene products represent potential new compounds that are inhibitory to the bacterial pathogen and thus useful as pharmaceuticals. The utility of this concept is demonstrated in the missing gene for lysine decarboxylase, and the resulting inhibitory activity of cadaverine (the diaminoalkyl reaction product of lysine decarboxylase) on the Shigella enterotoxins. Diaminoalkyl compounds are therefore potent inhibitors of E. coli and Shigella spp. enterotoxins. Lysine decarboxylase generated from the gene cadA results in attenuation of the enterotoxic effects. New methods of use of diaminoalkyl compounds as medicaments are described. New uses of genetic constructs containing a cadA sequence, or other 'anti-virulence' gene, for biochemical probes, for toxin receptor identification, and for pharmaceutical discovery are described. Additional uses are described for vaccines and DNA vaccine delivery.
US20090076034 Deuterium-enriched bms-690514 The present application describes deuterium-enriched BMS-690514, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2014134313A1 Intermediates for use in the preparation of indazole derivatives and processes for the preparation thereof Provided herein are novel processes for preparing a compound of Formula (I) to the use of said compound as an intermediate in novel processes for the synthesis of indazole derivatives, and to indazole intermediates and derivatives prepared by the processes described herein.
CN101177433B (s)-ornidazole disodium phosphate pentahydrate as well as preparation method and uses thereof The invention relates to a levo ornidazole disodium pentahydrate, which can be used for preparation of tablets, capsules and intravenously-delivered drugs, and treatment of infection due to sensitive archaeorganism and anti-anaerobic bacteria. The invention has the advantages of better stability, higher bioavailability and better efficacy compared with non-hydrate.
US20080171715 Administering synthetic miRNA or inhibitor as an anticarcinogenic agent that protects noncancerous cells and is effective against chemo- and radiation resistant cancer cells; breast, colon, thyroid and lung cancers; antimetastasis agents The present invention concerns methods and compositions for introducing miRNA activity or function into cells using synthetic nucleic acid molecules. Moreover, the present invention concerns methods and compositions for identifying miRNAs with specific cellular functions that are relevant to therapeutic, diagnostic, and prognostic applications wherein synthetic miRNAs and/or miRNA inhibitors are used in library screening assays.
CN103356628A Use of pyrazolopyrimidine compound in pharmacy The invention relates to a use of a pyrazolopyrimidine compound in treatment on candida albicans-infected diseases. The pyrazolopyrimidine compound is N3-(4-fluoropentyl)-1H-pyrazolo[3,4-D]pyrimidine-3,4-diamine. The pyrazolopyrimidine compound has good activity of resisting various shallow and deep fungi. Compared with the existing antifungal drugs in clinical application, the pyrazolopyrimidine compound has the advantages of high efficiency, low toxicity and wide antifungal spectrum and can be used for preparation of antifungal drugs.
CN101416978A Preparation method of tilmicosin long-acting injection The invention discloses a preparation method of a tilmicosin long acting injection, which comprises the following steps: (1) 10g to 20g of tilmicosin is accurately weighed and put into a beaker; (2) 25ml to 75ml of propylene glycol is taken by a measuring cylinder, poured into the tilmicosin, stirred, put and fully dissolved in a water bath with the temperature of 60 DEG C, and then water used for injection is added; (3) the pH value is regulated to be 5.5 to 6.5 by phosphoric acid; (4) the volume is fixed to be 100ml by the measuring cylinder; and (5) after filtering and encapsulation, sterilization is carried out at the temperature of 100 DEG C for 30min; and the finished product is obtained after cooling, light inspection, printing and packaging. The veterinary drug has the advantages of advanced production technique, stable preparation, long storage life, quick effect, long half-life period up to 2 days to 3 days, safe use, exact therapeutic effect, convenient application and the like.
WO2007092496A3 7,9-dihydro-purin-8-one and related analogs as hsp90-inhibitors The invention relates in general to 7,9-dihydro-purin-8-one and related compounds that show broad utility, e.g., in inhibiting heat shock protein 90 (HSP90) to thereby treat or prevent HSP90-mediated diseases.
CN101987105A Compound preparation for treating diseases caused by poultry sensitive bacteria and preparation method thereof The invention relates to a compound preparation for treating diseases caused by poultry sensitive bacteria and a preparation method thereof. The compound preparation is a long-acting injectable suspension prepared from florfenicol and occrycetin as main medicines and comprises 2.0-20.0% (W/V) of florfenicol, 5.0-30.0% (W/V) of occrycetin, 0.05-0.40% (W/V) of antioxidant, 1-10% (W/V) of antiallergic factor synergist, 0.01-0.04% (W/V) of complexing agent, 0.01-15% (W/V) of suspending agent, 1.0-10.0% (W/V) of flocculating agent, 0.01-0.5% (W/V) of preservative and 60-100% (W/V) of water for injection. The liquid medicine of the invention has stable performance and can effectively overcome the defects of instable performance, easy color change, precipitation and failure and the like of injections. The compound preparation has small irritativeness, low cost and simple process and can prolong the residence time of medicine in body and increase the bioavailability of the medicine. The compound preparation can be used for preventing and treating infectious diseases caused by poultry sensitive bacteria, such as pasteurellosis, colibacillosis, salmonellosis, contagious pleuropneumonia, mycoplasmlpneumonia of swine, acute respiratory infection and the like.
CN102106882A Natural compound medicine for treating acnes and scars The invention provides a pharmaceutical composition for treating acnes and scars. The pharmaceutical composition contains cryptotanshinone and centella selected triterpenes, and can be prepared into a dosage form such as an oral preparation or an external preparation. In the invention, a pharmacodynamics contrast test is carried out, wherein a tanshinone extract, the centella selected triterpenes and combination thereof are compared with three pharmaceutical compositions in the invention, and two dosage forms of capsules and cream are compared with each other. A plurality of test results prove that the pharmaceutical composition provided by the invention is respectively superior to two single-component preparations and combination of the two drugs, and has an obvious curative effect on acnes and scars.
US20100022598 Substituted inmidazoles as bombesin receptor subtype-3 modulators Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
CN1579402A Medicinal composition for treating bacterial conjunctivitis and keratitis and preparation and preparation method The invention provides a medicine compound and its manufacturing method, concretely, it is slow released eye preparation containing hydrochloric acid levo ofloxacin and its manufacturing method. The invention uses in situ gelling technology to produce the eye drip, the quality is stable, and it can maintain effect medicine density in a long time, upgrades the biological utilization rate, reduces the stimulation to eyes, reduces the medicine feeding frequency, the producing process is high controlled, the cost is low, it provides a new medicine for clinic.
CN102600175A Application of ursolic acid in medicament for treating neoplastic diseases The invention discloses a preparation method of ursolic acid and application of the ursolic acid in a medicament for treating neoplastic diseases. The molecular formula of the ursolic acid is C30H48O3, and the molecular weight of the ursolic acid is 456. The preparation method of the ursolic acid comprises the steps of drying and wholly crushing oldenlandia diffusa (taken as raw material), extracting the crushed oldenlandia diffusa by using ethyl acetate and ethanol respectively, combining the obtained extract, then separating the obtained extract by a normal-phase column and an RP-C18 reversed-phase column, then collecting by adopting a counter-current chromatography separation system of normal hexane-ethyl acetate-carbinol-water, and volatilizing a solvent to obtain ursolic acid monomers. The ursolic acid prepared by the invention is taken as a single-ingredient preparation or is combined with medical dressing, and has obvious antineoplastic activity on drug-resistance cells of the cancer of liver, the mechanism of action of the ursolic acid is a caspase non-dependence cell apoptosis pathway mediated by AIF (Apoptosis Inducing Factor). The ursolic acid has low toxicity and thus has good application prospects in clinical tumor chemotherapy and particularly multidrug resistance of clinical tumor chemotherapy.
US7947705 7-azaindoles and the use thereof as therapeutic agents The invention relates to substituted 7-azaindoles, process for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of phosphodiesterase 4 activity in particular in immunocompetent cells (e.g. macrophages and lymphocytes) by the compounds of the invention.
US7595316 2-(1-Cyclopentylpiperidin-4-yloxy)-5-(4-cyanophenyl)pyrimidine, for example; exhibits histamine receptor H3 antagonist or inverse agonist activity and is useful for the treatment and/or prevention of obesity, diabetes, hormonal secretion abnormality, sleep disorders Compound of the formula: (I) [wherein each of X1, X2 and X3 independently represents N or CH, W represents the formula (II):(II) or the formula (III):(III) and Y represents a group of the formula (IV):(IV)], or a pharmacologically acceptable salt thereof. This compound exhibits histamine receptor H3 antagonist or inverse agonist activity and is useful of the treatment and/or prevention of obesity, diabetes, hormonal secretion abnormality, sleep, disorder, etc.
US6849625 Use in manufacture of a medicament for use as an anti-invasive agent in containment and/or treatment of solid tumor disease The invention concerns quinazoline derivatives of Formula I wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
US20120309713 N-Cyclopropyl-(20R)-2-Methylene-19,26,27-Trinor-25-Aza-Vitamin D Analogs and Their Uses This invention discloses N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs, and specifically N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-1α-hydroxyvitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
CN102160854A Cyclodextrin-included florfenicol quick-release water-soluble powder preparation and preparation method thereof The invention relates to a cyclodextrin-included florfenicol quick-release water-soluble powder preparation and a preparation method thereof. The preparation is prepared by stirring florfenicol, cyclodextrin and water at a uniform speed and including by using an inclusion technology. The preparation can be directly dissolved in water to be taken by livestock, and has the characteristics of high medicine dissolution rate, high dissolubility, high bioavailability, good absorption and the like; and the medicine (florfenicol) is included in a carrier material, the bitterness of the florfenicol can be masked, and the intake or drinking of animals cannot be influenced by the bitterness of the medicine.
US20090035355 Confectionery products and process for obtaining them Agglomerates comprising calcium-hydrocolloid-composite materials and at least one sugar alcohol, as well of methods for preparing the agglomerates and various applications thereof.
CN103751173A Application of dihydromyricetin in preparation of liver regeneration medicine The invention relates to the biomedical field, and particularly relates to application of dihydromyricetin in preparation of a liver treatment and regeneration promotion medicine. Dihydromyricetin shows relatively high oxidation resistance and characteristic on promoting cell growth as a flavonoid compound. The test shows that dihydromyricetin can effectively relieve liver tissue necrosis caused by acute hepatic failure and can promote hepatocyte proliferation, so as to obviously raise the survival rate of a model mouse suffering from acute hepatic failure; dihydromyricetin also can obviously improve the activity of superoxide dismutase in tissue and serum, increase the content of serum protein, and lower down the levels of glutamic oxalacetic transaminase, glutamic-pyruvic transaminase and tumor necrosis factor alpha.
CA2449217C Process for cleaning hard gelatine capsules The invention relates to a process which can be used in the laboratory or on an industrial scale for cleaning the inner wall of hard gelatine capsules, in which the sealed capsules are cleaned with a powder formulation.
US20060029663 Solid formulation (wherein R1, R2 and R3 may be the same or different and each represents a hydrogen atom, lower alkyl, lower alkenyl or lower alkynyl; and R4 represents cycloalkyl, —(CH2)n—R5 or the above formula (II)) The present invention provides a solid formulation comprising a xanthine derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof, and microcrystalline cellulose, which possesses excellent pharmaceutical properties, for example, in hardness, disintegration property, dissolution property, stability or the like.
US20100104507 Use of sterically stabilized cationic liposomes to efficiently deliver cpg oligonucleotides in vivo Sterically stabilized cationic liposomes (SSCL) encapsulating a K type oligodeoxynucleotide (ODN) including a CpG motif are disclosed. These SSCL encapuslating a K type ODN can be used to effectively deliver the ODN to a cell. A novel method is also disclosed for producing the SSCL encapsulating the K type ODN. Administration of the SSCL encapsulating a K type ODN and a chemotherapeutic agent, such as a chimeric molecule comprising a targeting molecule selected from the group consisting of an IL-13, and an anti-IL-13 receptor antibody; and an effector molecule selected from the group consisting of a Pseudomonas exotoxin, a Diphtheria toxin, and a radionuclide, can be used to dramatically reduce the growth of solid tumors.
WO2006105127A2 Hydroxysteroid dehydrogenase inhibitors Compounds, pharmaceutical compositions, kits and methods are provided for use with hydroxysteroid dehydrogenases that comprise a compound selected from the group consisting of: formula (I), wherein the variables are as defined herein.
CN101676255A Synthetic method of iodized vegetable fatty acids and their esters The invention relates to a synthetic method of iodized vegetable fatty acids and their esters. In the invention, at first, vegetable fatty acids are prepared from vegetable oils by the saponificationand acidification, the fatty acids are in the iodination reaction with phosphorus trichloride, phosphorous oxychloride or phosphorus pentachloride and alkali metal iodides such as sodium iodide and the like in an organic medium in the presence of water to generate a hydroiodic acid on site. The iodized vegetable fatty acids are reacted with the alcohol in the catalysis of the acid to produce iodized vegetable fatty acid esters.
CA2661800A1 Bifeprunox doses for treating schizophrenia The present disclosure is directed to a daily dose of bifeprunox for the treatment of a patient with schizophrenia. Such dose is effectively used in methods for treating schizophrenia comprising administering to a patient a pharmaceutical composition comprising an effective amount of at least one bifeprunox compound, amongst other effects, resulting in a reduction of side effects associated with schizophrenia treatment such as: no weight gain, improvement of non-fasting triglyceride levels and/or total cholesterol levels. Treatment effects are e.g. a reduction of PANSS total score in a patient and an increase of the time to deterioration of schizophrenia and improvement of psychotic symptoms.
US20120029062 Interior functionalized hyperbranched dendron-conjugated nanoparticles and uses thereof Provided herein are nanoparticle platforms and combinatorial drug delivery vehicles comprising gold nanoparticles with a plurality of thilolated hyperbranched dendrons conjugated to the nanoparticle surface. The thiolated hyperbranched dendrons comprise chemically-modifiable surface groups, functionalized interior groups and nano-cavities within the hyperbranched structure to which a variety of payload molecules may be conjugated, optionally via a linker. Payload molecules may comprise nucleic acids, anticancer drugs and small molecule inhibitors, optionally with, non-cytotoxic signaling agents, for example, fluoroscein isothiocyanate. Also provided are methods for delivering one or more therapeutic agents to a cell or tissue or for treating a pathophysiological condition in a subject by delivering the combinatorial drug delivery vehicles to a cell or tissue associated with the pathophysiological condition to facilitate internalization of the vehicle to effect treatment.
WO2013162027A1 Neuronal differentiation promoter The present invention provides a neuronal differentiation promoter for a neural stem cell, which comprises a p38 inhibitor. The present invention also provides a method for promoting the neuronal differentiation of a neural stem cell, which comprises culturing the neural stem cell in the presence of a p38 inhibitor. The neural stem cell is of a gliogenesis type of a neurogenesis type. The p38 inhibitor is a nucleic acid that can hybridize with DNA encoding p38 or mRNA for the DNA under physiological conditions to inhibit the transcription and/or translation of the DNA or the mRNA, an expression vector for the nucleic acid, a low-molecular-weight p38 inhibitor or the like.
WO2012129564A3 Proteasome chymotrypsin-like inhibition using pi-1833 analogs Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e. substitution of one of the hydrogens by methyl) demonstrated chiral discrimination in proteasome CT-L activity inhibition (the S-enantiomer was 35-40 fold more potent than the R-enantiomer).
US20080306020 Skin-Protecting Alkalinity-Controlling Composition and the Use Thereof A skin-protecting alkalinity-controlling composition comprises one or more carboxylic acid polysaccharides. Said compositions are capable of providing buffering, and thus avoiding a major increase in the pH of an aqueous system and/or are capable of reducing the pH of aqueous systems, in which alkalinity is formed as a result of chemical and/or biological reactions. The compositions may be used in personal care products, such as skin creams and lotions, hygiene products, wound care products, fabric treating products etc.
US20120165304 6,7,8,9-Tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them The present invention relates to compounds defined by formula (I), wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.
CN103735551A Pharmaceutical composition for heart and cerebral vessels as well as preparation method and application of pharmaceutical composition The invention relates to a pharmaceutical composition of ticagrelor and a type II therapeutic agent and a preparation method of the pharmaceutical composition. The pharmaceutical composition is characterized in that the type II therapeutic agent is selected from one or more of troxerutin, cinnarizine, flunarizine hydrochloride, ligustrazine, ligustrazine phosphate, sodium ferulate or piperazine ferulate. The invention also relates to application of the pharmaceutical composition in drugs, in particular the application in inhibiting or reversing of atherosclerosis lipid plaques of artery blood vessel.
CN102579324A Application of levetiracetam injection in preparation of nootropic drugs The invention relates to an application of levetiracetam injection in preparation of nootropic drugs. At present, levetiracetam is an antiepileptic drug with a very good curative effect, and researches find that the drug has a better curative effect in the nootropic aspect. The invention aims to further explore the application of the levetiracetam injection in the nootropic aspect, which has the advantages of quick drug effect, strong practicability and storability, compared with oral preparations.
US20080107742 Alkalinizing agent, humectant, detergent, wetting agent, antibacterial agent, stabilizer, emulsifier, antifungal agent, colorants, moisturizer, thickening agent, preservative, filler, keratolytic agent; menthol, camphor counterirritants; granules, beads, microspheres, grit, pumice, polymer, sand, glass The present application is directed to various compositions to treat the itching and conditions that result from contracting poison ivy, poison oak, and poison sumac, as well as other plant and substances that contain substances that lead to a skin reaction but that upon removal alleviate the symptoms of the condition. In particular, the compositions described herein are useful for removing urushiol after it has contacted the skin. The compositions include granules or other scrubbing means to reach the urushiol in the skin, a mixture of surfactants to form a complex with the urushiol, counter-irritants to provide a soothing sensation to the irritated skin, and other functional ingredients to provide additional benefits to the individual who has contacted urushiol.
CN103705500A Applications of Myrtucommuacetalone in medicines treating renal insufficiency The invention discloses applications of Myrtucommuacetalone in medicines preventing and/or treating renal insufficiency, belongs to the technical field of new applications of medicines, and is disclosed for the first time. The skeleton type belongs to a brand new skeleton type. Myrtucommuacetalone has strong inhibition activity to renal insufficiency, has outstanding substantive features and has substantial progress in controlling renal insufficiency obviously.
EP1442024B1 AMINOBENZAMIDE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3$g(b) INHIBITORS This invention concerns a compound of formula (I),a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C¿1-6?alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R?2¿ is hydrogen, C¿1-10?alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R?3¿ is hydrogen; hydroxy; halo; optionally substituted C¿1-6?alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R?21; R21-C¿1-6alkyl; R?21-O-; R21-S-; R21¿-C(=O)-; R21-S(=O)¿p-; R?7-S(=O)¿p-; R?7-S(=O)¿p?-NH-; R?21¿-S(=O)¿p?-NH-; R?7¿-C(=O)-; -NHC(=O)H; -C(=O)NHNH¿2; R?7-C(=O)-NH-; R21-C(=O)-NH-; -C(=NH)R7; -C(=NH)R?21 ; R4a or R4b¿ each independently represent hydrogen, R8, -Y1-NR9-Y2-NR?10R11, -Y¿1-NR9-Y1-R8, -Y1-NR9R10; provided that -X-R2 and/or R3 is other than hydrogen;their use, pharmaceutical compositions comprising them and processes for their preparation.
WO2006105313A2 Compositions of and methods of using oversulfated glycosaminoglycans The invention relates, in part, to compositions comprising glycosaminoglycans, fragments of glycosaminoglycans or glycosaminoglycan fractions. The compositions provided can be used in various methods of modulating FGF and/or VEGF activitity. The method can be in vitro or in vivo methods. Therefore, the invention also relates, in part, to methods of treating a subject with the compositions provided.
WO2006082063A3 Cpg-odn (oligodeoxynucleotides) with stem-loop and flanking sequences without cpg-motifs for the treatment of skin diseases The invention relates to: cosmetic or pharmaceutical preparations, for preventing and/or treating epithelial tegument, that contain nucleic acids, which have sequences suited for forming stem-loop secondary structures; the use of nucleic acids of this type, which have sequences suited for forming stem-loop secondary structures, for preventing and/or treating epithelial tegument and; fabric softeners, hand detergents, body and hair care products, hair coloring agents or hand dishwashing detergents containing these nucleic acids that have sequences suited for forming stem-loop secondary structures.
WO2014074846A1 Methods for the treatment of bone loss Provided herein are methods of treating, preventing and/or managing bone loss using (+)-2- [ 1 -(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-4-acetylaminoisoindolin- 1,3-dione, alone or in combination with other therapeutics.
CN103599111A Combined drug for treating pancreatic cancer The invention discloses a combined drug preparation for treating pancreatic cancer. Withaferin A and oxaliplatin are used by the combined drug preparation for treating the pancreatic cancer. The Withaferin A and oxaliplatin can be used for killing cancer cells through oxidative stress injury mediated by the ROS (reactive oxygen species), two ROS in different sources can be united to develop the synergistic effect after combined medication, and the effect of killing pancreatic cancer cells is obvious stronger than that of single medication. Under the concentration in which the combined drug does not generate obvious toxic effect on the normal cells, the growth inhibiting effect of the combined drug on the pancreatic cancer cells is more obvious than that of clinical first drugs gemcitabine for the pancreatic cancer, the result shows that the combined drug can be well applied to treatment of the pancreatic cancer and preparation of the drugs for treating the pancreatic cancer.
US20100322992 Anti-Proliferative And Anti-Inflammatory Agent Combination For Treatment Of Vascular Disorders With An Implantable Medical Device Drug-delivery systems such as drug-delivery stents having an anti-proliferative agent such as everolimus and an anti-flammatory agent such as clobetasol are provided. Also disclosed are methods of treating a vascular impairment such as restenosis or vulnerable plaque
WO2013139274A1 Sodium pyruvate oral rehydration salt composition for treating hypovolemia or hyponatration associated with hypohydration Disclosed in the present invention is a sodium pyruvate oral rehydration salt composition for treating hypovolemia or hyponatration associated with hypohydration, said composition containing the following components: (i) 2.0-6.0 parts by weight of sodium pyruvate; (ii) 1.5-17.0 parts by weight of sodium chloride; (iii) 0-2.0 parts by weight of potassium chloride; (iv) 10.0-50.0 parts by weight of glucose anhydrous or other carbohydrate. The weight of components (i) + (ii) + (iii) + (iv) constitutes 50-100% of the total weight of the composition.
CN101053618A Ointment for treating hyperplasia carbuncle wound and its preparing process The invention relates to a medicinal ointment for treating furuncle comprising angelica, prepared rehmannia root, dried rehamnnia root, giant typhomium tuber, dog button, momordica seed, croton seed, pangolin, cassia bark, centipede, scorpion, frankincense, myrrh, bezoar, musk, bornel, minium, balm, moreover, dragons blood, peach kernel, pubescent angelica root, Piper hancei Maxim., burred tuber and zedoary may also be added. The invention can treat traumatic injury, ulcer and various hyperplasia conditions.
CN1823774A Domperidone drip pills and its preparation method A dripping pill of domperidone for treating indigestion, nausea, vomiting, etc is prepared from domperidone and matrix.
WO2005019190A3 (4 -amino -1,2, 5-oxadiazol-4-yl) -hetξroaromatic compounds useful as protein kinase inhibitors The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. In certain embodiments, these compounds are effective as inhibitors of p70S6k, GSK- 3 and/or ROCK protein kinases. These compounds have the general formula I.
US20100255069 Compositions and methods for treating angiogenesis-related diseases, wounds and cosmetic use of components of angelica sinensis, and methods of preparation thereof Compositions and methods for treating angiogenesis-related diseases and for skin care in mammals is disclosed that includes, as an active pharmaceutical agent, an effective amount of purified extract from Angelica sinensis, or a fraction or a lyophilizate thereof, or one or more active component contained in said extract.
US20080300266 metabotropic glutamate receptor (mGluR3) antagonists such as [1-(5-bromopyrimidin-2-yl)-pyrrolidin-3-yl]-(2,4-dichlorobenzyl)-amine, used for the treatment of depression, schizophrenia and headaches The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.
US20110086849 novel benzoxazine benzimidazole derivative, a pharmaceutical composition comprising the same, and ause thereof The present invention relates to a novel benzoxazine benzimidazole derivative of formula (1) as an antagonist against a vanilloid receptor-1, a pharmaceutical composition comprising the same as an active ingredient, and a use thereof. The benzoxazine benzimidazole derivative of the present invention may be useful for preventing or treating a disease associated with antagonistic activity of vanilloid receptor-1: wherein, R1, R2, R3, R3′, Q1, Q2, Q3 and Q4 have same meanings as defined in the specification.
EP1699788A2 Imidazoquinolinyl, imidazopyridinyl and imidazonaphthyridinyl sulfonamides Imidazoquinolinyl, imidazopyridinyl, and imidazonaphthyridinyl sulfonamide compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
US7754757 Dipeptidylpeptidase IV (DPP-IV) inhibitory activity; (2S,4S)-1-[[N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)); diabetes Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).
CN101428038A Powder preparation for quick cicatrization of incised wound The invention relates to a powder for rapidly healing an incised wound. The powder is prepared by the following bulk drugs (parts by weight): 10g-50g of quicklime and 10-50g of rat (one), and the preparation method comprises the following steps: the rat and the quicklime are mixed to be ground into powder for standby application. The invention has the advantages that firstly, the powder is applied to the wound, and the incised wound can be rapidly healed; and secondly, the preservation and the carrying of the powder are convenient.
CN1628665A Levobupivacaine freeze dried for injection and preparation method thereof The invention relates to Levobupivacaine freeze dried injection and its preparation method, which comprises treating effective amount of pharmaceutically acceptable salt of Levobupivacaine and freeze dryable adjuvant, wherein each preparation unit contains Levobupivacaine pharmaceutically acceptable salt 10-300mg. the freeze dryable adjuvant includes diluent, isotonic conditioning agent, pH modifier.
CN1711279B Epstein Barr virus peptide epitopes, polyepitopes and delivery system therefor Immunogenic cytotoxic T cell epitope peptides of Epstein Barr Virus LMP1 protein are provided having between nine and seventeen amino acids and minimal consensus sequences selected from QRH, AGNDG, QNW, VLYS and DSNSNE. These peptides, either individually or in polyepitope constructs, are useful in pharmaceutical compositions, vaccines and methods of treating Epstein Barr Virus associated diseasessuch as Hodgkin's Disease and/or Nasopharyngeal Carcinoma, although without limitation thereto. A preferred mode of polyepitope delivery is an adenovirus-based system.
CN101239072B Medicaments for treating syphilis disease and preparation thereof The invention relates to a medicine for curing syphilis, which is prepared with 6 to 9 shares of borneol, 6 to 9 shares of white vitriol, 3 to 5 shares of cinnabar, 2 to 4 shares of mercury, 4 to 6 shares of sal ammoniac and 4 to 6 shares of saltpeter. The method adopted by the invention to prepare the medicine is that the raw materials which are covered by a new porcelain bowl, then sealed and placed in a pot are heated on a small fire for 30 to 50 munities and then on a large fire for 90 to 110 munities, and then the powder in the bowl is collected after the pot is cooled down. The medicineprovided by the invention is small in terms of toxic and side effect, convenient to use, short in terms of curing time, remarkable in terms of curing effect and low in cost.
CN101353664A siRNA molecule expression vector for specific inhibition of IL-6 receptor protein expression, and construction method and use thereof The invention discloses a small interfering RNA molecule expression vector which inhibits the expression of IL-6 receptor protein specifically and a construction method and application thereof; the invention aims at providing a small interfering RNA molecule expression vector which inhibits the expression of IL-6 receptor gene and application thereof as clinical therapeutic drugs; the small interfering RNA is double-stranded sequence, wherein, the SODN of the small interfering RNA is SEQ ID NO: 1 in the sequence list and the antise strand is SEQ ID NO: 2; or is other nucleotide sequence which is designed according to the principle stated in the instruction and is from the coding area of the IL-6 receptor gene; the constructed small molecular interfering RNA expression vector can be used for curing the relevant symptoms caused by ectopic expression of the IL-6 receptor genes. The small interfering RNA molecule expression vector of the invention has larger application value and prospect in the field of medicine and biological pharmacy.
WO2014015276A1 α-AND γ-TRUXILLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF The present invention provides a compound, and method of inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, having the structure: Formula (I).
US20050054632 Naphthyl compounds, intermediates, compositions, and methods of use The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.
WO2007113243A2 Use of pde 5 inhibitors for the treatment of overactive bladder The present invention relates to the use of an inhibitor of cyclic guanosine 3', 5'-monophosphate-specific phosphodiesterase type 5 (PDE 5) activity or of an inhibitor of PDE 5 expression for the manufacture of a medicament for the treatment and/or prophylaxis of overactive bladder disease. In addition, it further refers to pharmaceutical compositions containing said inhibitors of PDE 5 activity and expression.
US20110305764 Use of a Mare's Milk Concentrate Dried on a Highly-Dispersed, Biologically Inert Matrix The invention relates to the use of a mare's milk concentrate dried on a highly-dispersed, biologically inert matrix, for producing a preparation for the treatment of skin diseases, especially dry skin diseases.
US6992105 N-[2-[(S)-2-Acetylthio-3-methylbutanoylamino]-2-methylpropionyl]-O-ben-zyl-L-serine Ethyl; inhibitors of angiotensin converting enzyme, neutral endopeptidase, endothelin converting enzyme. Compounds of the formula wherein R, R1, COOR2, R3–R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.
US20110165141 Compositions for treating bacterial infections Polynucleotides encoding a mutant human carboxylesterase enzyme and polypeptides encoded by the polynucleotides which are capable of metabolizing a prodrug and inactive metabolites thereof to active drug are provided. Compositions and methods for sensitizing cells to a prodrug agent, inhibiting cell growth, treating drug addiction, and facilitating the metabolism of an organophosphate with this enzyme are also provided. In addition, a screening assay for identification of drugs activated by this enzyme is described.
US7232906 Kinase inhibitors; antiinflammatory agents; respiratory system disorders; cardiovascular disorders; antidiabetic agents The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
WO2012156284A1 1,3-oxazines as bace1 and/or bace2 inhibitors The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
EP1399173B1 Pharmaceutical preparation containing active ingredients extracted from the plants centella asiatica, mahonia aquifolium and viola tricolor The invention relates to the use of a pharmaceutical preparation for producing a medicament used for treating allergic skin diseases, atopic eczema, skin diseases caused by fungi, urticaria, neurodermatitis, psoriasis, psora, skin eczemas, pruritus of the skin, inflammatory skin diseases and/or viral diseases, including chickenpox, varicellas, herpes and herpes zoster. The inventive pharmaceutical preparation comprises natural and/or synthetic active ingredient(s) extracted from the plants Centella asiatica, Mahonia aquifolium, Viola tricolor and/or from plant parts thereof.
CN1974576A N1,N8-disubstituent-triethyl tetramine copper (II) complex and its prepn process The present invention relates to N1, N8-disubstitutent-triethyl tetramine copper (II) complex as one kind of small molecular polyamine metal complex. Research shows that N1, N8-disubstitutent-triethyl tetramine copper (II) complex may be combined with DNA at the major groove in the insertion mode, the DFT process confirms the action mode between the complex and DNA, gel electrophoresis process shows that the complex can incise DNA, and MTT process proves the cancer cell inhibiting effect of the complex, so that the complex may be used in developing effective chemical nuclease and high efficiency and low toxicity anticancer medicine.
CN102258459B Rosuvastatin calcium oral solid preparation and applications thereof The invention relates to a rosuvastatin calcium oral solid preparation and applications thereof. The rosuvastatin calcium oral solid preparation is prepared in tablets and capsules by a solid dispersion technology so as to increase the stability of the preparation, simultaneously enable the medicine to be released slowly and continuously and further effectively avoid the adverse effect caused by peak-valley fluctuation of the blood concentration.
WO2007058392A1 Heterocyclic compound and medicinal application thereof It is intended to provide a novel heterocyclic compound having an HCV entry inhibition activity and a medicinal application thereof. The invention relates to the use of the heterocyclic compound represented by the general formula [1]: [wherein Q1 represents N= or the like, Q2 represents N or the like, Q3 represents N= or the like, Q4 represents N or the like, Q5 represents N or the like, R1 represents a hydrogen atom or the like, R2 represents a hydrogen atom or the like, the ring A represents a monocyclic aryl group which may have a substituent or the like and the ring B represents a monocyclic aryl group which may have a substituent or the like], a pharmaceutically acceptable salt thereof for the production of a therapeutic agent for hepatitis C and so on.
CN103156803A Ketoprofen gel and preparation method thereof The invention relates to a ketoprofen gel and a preparation method thereof. The ketoprofen gel is prepared from the following components: 2-5 % of ketoprofen, 0.5-2 % of matrix material, 2-4 % of a transdermal enhancer, 0.5-5 % of a neutralizer, 0.05-0.2 % of an anti-oxidant, 20-50 % of ethanol and the balance being water. The ketoprofen gel provided by the invention solves problems of stimulation of ketoprofen preparations on gastrointestinal tract in a background technology, is used externally, has advantages of good transdermal effect, quick effect and good analgesic and anti-inflammatory effects, and can play drug effects for a long time.
CN101328200B Antineoplastic compound, preparation and use thereof The invention relates to a novel triterpene alkaloid compound, namely Buxus microphylla G with a structural formula as shown on the right, a preparation method thereof, a medical composition taking a Buxus microphylla G compound as an active ingredient, and an application of the Buxus microphylla G in treating tumor disease.
US20100286084 Oligomer-Nucleoside Phosphate Conjugates The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble, non-peptidic oligomer. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
US20090029961 Bio-Film Resistant Surfaces The present invention relates to methods and compositions for rendering a surface resistant to bio-film formation by a combination of an alkanediol and an antimicrobial agent (and, optionally, an organic hydroxy acid). The invention provides for compositions which may be used to render surfaces bio-film resistant, articles having bio-film resistant surfaces, and methods for their preparation. The present invention may be advantageously applied to medical articles as well as articles used in non-medical contexts, such as child care or food preparation.
EP2590956A1 5-(biphenyl-4-yl)-3-phenyl-1,2,4-oxadiazolyl derivatives as ligands on the sphingosine 1-phosphate (s1p) receptors The present invention provides compounds of Formula (I), as selective S1 P1 inhibitors, as well as their use for treating multiple sclerosis and other diseases.
WO2014027669A1 Pyrroloquinoline quinone tetraalkali salt, crystals thereof, method for manufacturing same, and composition The purpose of the present invention is to provide a pyrroloquinoline quinone tetraalkali salt, crystals of pyrroloquinoline quinone tetraalkali salt, a composition, and a simple method for manufacturing high quality, high purity pyrroloquinoline quinone tetraalkali salt that does not require a special reagent, has high solubility in a solvent, allows a pyrroloquinoline quinone aqueous solution to be obtained in high concentration, and in which discoloration is not liable to occur even when used to together with ascorbic acid. A pyrroloquinoline quinone tetraalkali salt represented by formula (1) (wherein, M is at least one element selected from the group consisting of, independently, Li, K, Na, Rb, and Cs)
CN103393182A Health-care fruit oral liquid for pregnant women The invention discloses health-care fruit oral liquid for pregnant women. The oral liquid is characterized by being prepared from the following raw materials in parts by weight: 30-50 parts of brown sugar, 10-15 parts of fresh grape, 5-10 parts of dried red date, 3-6 parts of honeysuckle, 5-10 parts of longan aril, 5-10 parts of angelica and 5-10 parts of honey. According to the oral liquid, the fresh grape, the brown sugar, the angelica and the like are selected and used, so that the nutritive value of the product is multiplied; the nutritional requirement of the pregnant women can be provided, particularly the grape has an effect of effectively slowing down the edema of the pregnant women, and the dried red date, the brown sugar and the angelica provide rich vitamins, also have a blood enrichment function and are particularly suitable for meeting the female needs during the pregnancy.
CN103214472A Preparation of two novel non-ATP (Adenosine Triphosphate) competitive FGFR1 (Fibroblast Growth Factor Receptor1) inhibitors and anti-tumor activity of two novel non-ATP competitive FGFR1 inhibitors The invention provides FGFR1 (Fibroblast Growth Factor Receptor1) non-ATP (Adenosine Triphosphate) competitive inhibitor acrylamide compounds. Besides, the invention also provides a medicine composite of the compounds, anti-tumor application of the compounds, and the like.
US20120003198 Lutein/Zeaxanthin for glare protection The invention relates to the improvement of visual performance, particularly of visual performance in the darkness, by administration of a colorant that is capable of being incorporated into eye tissue and/or causing yellowing of eye tissue, especially carotenoids, such as lutein and zeaxanthin.
CN1785971A Benzoin kind lean uranium discharging promotor, its preparation method and use The present invention relates to a new-type lean uranium eccritic, its preparation method and application. The invented lean uranium eccritic is a water-soluble tetrahydroxydeoxybenzoin derivative. Said invention uses p-hydroxyphenylacetic acid and pyrogallic acid (pyrogallol) as raw material, and makes them produce reaction in BF3.Et2O to obtain 2.3.4.4í»-tetrahydroxydeoxybenzoin, then uses the concentrated sulfuric acid to make sulfonation and arbitrarily select formed salt so as to obtain the invented eccritic. It can be used for promoting excretion of lean uranium, and can be used for intramuscular injection.
CN103622953A Medication for treating kidney cyst The invention relates to a medication for treating kidney cyst. The primary chemical composition of the medication is Gallein, and the chemical formula is C20H12O7; the medication prepared by chemical synthesis is previously applied to the field of cardiac therapy, but is never applied to the field of treating kidney related diseases; according to the invention, the medication prepared by chemical synthesis is for the first time applied to treating the kidney cyst disease; the probability of kidney cyst of mice is effectively reduced once the medication is injected into the mice, and the livability of the mice is greatly increased; the medication prepared by chemical synthesis is the first medication ever proposed to aim at effectively treating kidney cyst, provides very valuable reference for completely curing the kind of stubborn disease in the future, and can benefit widespread kidney cyst patients.
CN101343275A Preparation for pyrazole-pyrimidinethiones and its salt, and application of the same in treating mankind erection dysfunctional The invention relates to the preparation of pyrazole-pyrimidine thioketone as well as applications of salt thereof in curing male erectile dysfunction.
US20050124685 Polyether brevetoxin derivatives as a treatment for neurotoxic shellfish poisoning and ciguatera fish poisoning Disclosed are compounds that are derivatives of brevetoxin, or PbTx, pharmaceutical formulations comprising the compounds, and methods of administering the compounds to a subject for the treatment of neurotoxic shellfish poisoning or ciguatera fish poisoning, wherein the compounds have general Formulas (I) and (III): wherein R, R1, R2, R3, A, n, and Y are as defined herein for each compound.
WO2013084532A1 Prophylactic or therapeutic agent for dysuria The present invention provides a prophylactic or therapeutic agent for dysuria which comprises, as the active ingredient, prosultiamine, fursultiamine, a metabolite thereof, or a pharmaceutically acceptable salt thereof.
CN103120698A Application of triterpenoid saponins compound in preparation of anti-pathogenic microorganism medicines The invention provides application of a triterpenoid saponins compound in preparation of anti-pathogenic microorganism medicines, and in particular relates to application in preparation of antituberculous and anti-lepriasis medicines. The triterpenoid saponins compound is shown in a chemical formula described in the specification; in the chemical formula, any two of R1, R2 and R3 are methyl, while the other is hydrogen atom; R4 is pentabasic or hexabasic monosaccharide or disaccharide made of pentabasic or hexabasic monosaccharide, or glycosyl made of an aldehyde acid derivative of monosaccharide or disaccharide; R5 is hydrogen atom, or pentabasic or hexabasic monosaccharide or disaccharide made of pentabasic or hexabasic monosaccharide, or glycosyl made of an aldehyde acid derivative of monosaccharide or disaccharide, or a substituent made of the aldehyde acid derivative of monosaccharide or disaccharide. According to the invention, a medicine with remarkable anti-pathogenic microorganism effect is provided.
WO2009080301A1 Treatment and prevention of ischaemic cerebral lesions and cerebrovascular cognitive impairment using a treatment regimen consisting of dipyridamole and an angiotensin ii receptor blocker in patients with previous stroke The invention relates to a method of treatment or prevention of a condition selected from dementia and cerebral cognitive impairment, preferably due to white matter lesions as diagnosed by magnetic resonance imaging (MRI) of the brain, in a patient in need thereof, e.g. in patients with previous stroke or in elderly patients, comprising administering a therapeutically effective amount of dipyridamole (DIP) in combination with an angiotensin Il receptor blocker (ARB) and, preferably, in combination with a drug selected from other anti-platelet agents and/or a drug selected from the lipidlowering agents such as the statins to the patient.
CN103110622A Solid oral agent containing voglibose and atorvastatin calcium and preparation method thereof The invention discloses a solid oral agent containing voglibose and atorvastatin calcium. The solid oral agent contains the atorvastatin calcium, the voglibose, and pharmaceutically acceptable medicinal adjuvants, wherein the weight ratio of the atorvastatin calcium to the voglibose is (5-20):(0.1-0.4), and the adjuvants comprise one or more of starch, lactose, PVP (polyvinyl pyrrolidone), dextrin, microcrystalline cellulose, carboxy methyl cellulose, carboxymethyl starch sodium, hydroxypropyl cellulose, superfine silica gel powder, magnesium stearate. The invention also discloses a preparation method of the solid oral agent. The solid oral agent has the beneficial effects of synergistically improving the effects of reducing blood sugar and blood fat, correcting metabolic syndromes of diabetics, and being favorable for reducing the long-term risk of cardiovascular and cerebrovascular diseases of the diabetics.
CN102309497A Pharmaceutical composition for cardio cerebrovascular diseases A pharmaceutical composition for cardio cerebrovascular diseases comprises main components of ginsenoside Rd, puerarin and ferulic acid, and can be used to obviously minimize infarction area of brain tissues and obviously decrease behavior disorder due to brain tissue necrosis, thus achieving the purpose of treating insufficiency of cerebral blood supply, cerebral thrombus formation, cerebral infarction, cerebrovascular spasm, brain dysfunction, Alzheimer disease, parkinsons syndrome, cerebral stroke, hypertension, hyperlipidemia, arteriosclerosis, coronary heart disease, angina pectoris and myocardial infarction.
CN103417518A Application of oxidized resveratrol for preparing tumor treatment drugs The invention discloses an application of oxidized resveratrol for preparing tumor treatment drugs. Extracorporeal cell experiments indicate that the oxidized resveratrol has good growth inhibition effects on seven human source tumor cell strains including human leukemia cells K562, human ovarian carcinoma cells SK-OV-3, human breast cancer cells MCF-7, human hepatoma carcinoma cells SMMC-7721, human lung cancer cells A549, human nasopharyngeal carcinoma cells HNE-1 and human colon cancer cells SW480; the IC50 value of the oxidized resveratrol within 48 hours is between 0.047mM and 0.277mM; the growth inhibition effects on the human hepatoma carcinoma cells SMMC-7721, the human ovarian carcinoma cells SK-OV-3 and the human breast cancer cells MCF-7 are particularly obvious. Animal experiments indicate that the oxidized resveratrol has obvious inhibition effects on the growth of mouse transplanted tumor S180 sarcoma and mouse transplanted tumor H22 liver cancer, and is low in toxic and side effect.
WO2009138583A3 Use of a composition containing ergosterol or a natural extract of a vegetable or animal microorganism The invention relates to the cosmetic use or use as a food-additive of a composition that contains ergosterol, an ergosterol derivative, or a natural extract of vegetable or animal microorganisms containing the same in order to stimulate the natural defenses of cells, such as protein p53, against the consequences of an oxidative stress such as an exposure to ultraviolet, particularly solar, radiation, and in order to prevent the occurrence of senescent cells losing the reproductive capabilities thereof and having adverse effects on the surrounding tissues.
WO2014125444A1 Heterocyclic amides as kinase inhibitors Disclosed are compounds having the formula (I) wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
WO2012053758A2 Pharmaceutical composition for treating or preventing alcoholic liver diseases, containing cilostazol as active ingredient The present invention relates to a pharmaceutical composition for treating or preventing alcoholic liver diseases, containing cilostazol as an active ingredient. Particularly, cilostazol concentration-dependently inhibits the expression level of TNF-α and the genes of fatty acid synthase (FAS) and significantly inhibits the activity of caspase-3, thereby showing superior effects in treating or preventing alcoholic liver diseases, particularly alcoholic hepatitis, compared to pentoxifylline, which had been used as a therapeutic agent for alcoholic hepatitis, and thus can be used as a drug for treating or preventing alcoholic hepatitis.
US20080085885 Selective melanocortin-4 receptor agonist, dose dependently reducing ethanol self administration; alcoholism, alcohol abuse The present invention relates to methods of inhibiting or reducing voluntary alcohol consumption in a subject comprising administering a non-peptidyl melanocortin 4 receptor agonist to said subject. The present invention further relates to methods of treating or preventing alcoholism, alcohol abuse, and alcohol related disorders in a subject comprising administering a non-peptidyl melanocortin 4 receptor agonist to said subject. The present invention further provides for pharmaceutical compositions and medicaments useful in carrying out these methods.
WO2009075258A1 Transdermally absorptive preparation Disclosed is a tape-type transdermally absorptive preparation which has excellent transdermal absorption, high safety and high usability, and which is suitable for the treatment of a disorder of bone/calcium metabolism, such as osteoporosis, osseous Paget's disease and hypercalcemia associated with a malignant tumor. Specifically disclosed is a tape-type transdermally absorptive preparation characterized by containing a bisphosphonate or a derivative thereof. Preferably, the tape-type transdermally absorptive preparation comprises a support sheet and an adhesive layer laminated on one surface of the support sheet, wherein the adhesive sheet comprises: 100 parts by weight of an acrylic copolymer which comprises 50 to 88 wt% of acrylic acid, 8 to 40 wt% of 2-ethylhexyl acrylate and 1 to 42 wt% of a polar monomer (excluding acrylic acid); 150 to 600 parts by weight of a polyhydric alcohol; and a pharmaceutically effective amount of a bisphosphonate.
US20090023681 Method of using beta-glucan from schizophyllum commune Disclosed herein is a method for high-yield production of Schizophyllum commune-derived beta-glucan having a homogeneous composition, comprising subjecting mycelia of Schizophyllum commune to liquid culture with an addition of a synthetic adsorbent, and a composition for external application comprising the beta-glucan produced therefrom, which is capable of relieving dry skin conditions, atopic diseases and itching.
US20090326002 Thieno [2,3-b] Pyridine Compounds with mGluR Activity Provided herein are Thieno[2,3-b]pyridine compounds with mGluR activity. Also provided herein are processes and intermediates for the preparation of the Thieno[2,3-b]pyridine compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in treatment, therapy, and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.
CA2831426A1 Methods for increasing efficacy of folr1 cancer therapy Methods to improve the success of cancer therapies that target the human folate receptor 1 are provided. Kits comprising reagent useful in the methods are further provided.
CN102000059B Medicinal application of querecetin dipolymer flavonoids to preparation of glycosidase enzyme inhibitors The invention relates to medicinal application of querecetin dipolymer flavonoids to preparation of glycosidase enzyme inhibitors, in particular to medicinal application of querecetin dipolymer flavonoids or medicinal salts thereof to preparation of medicaments for inhibiting alpha-glucuroide and preventing and curing II type diabetes mellitus. The querecetin dipolymer flavonoids has very obviousactivity of inhibiting the alpha-glucuroide, and when the concentration of the querecetin dipolymer flavonoids is 4 mcg/ml, the alpha-glucuroide inhibiting strength of the querecetin dipolymer flavonoids reaches 75.0%; and the measurement on the half inhibiting concentration of the querecetin dipolymer flavonoids shows that the alpha-glucuroide inhibiting strength of the querecetin dipolymer flavonoids is 88 times of that of acarbose as a positive control medicament. The pharmacodynamics result indicates that the querecetin dipolymer flavonoids or the medicinal salts thereof can be expected to be used for preparing a glycosidase inhibitor medicament, and especially the medicaments for preventing and curing the II type diabetes mellitus.
US20080039529 Adjunctive Therapy for Depression This invention is directed to a method of treating depression in a subject, comprising the step of administering a therapeutically effective amount of a conventional antidepressant and, in addition, administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member Rx selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and 0 to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the oxygen atom.
WO2012143526A1 1,4-disubstituted 1,2,3-triazoles, methods for preparing same, and diagnostic and therapeutic uses thereof The present invention relates to a compound of general formula (I), where: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN' groups form, together with the carbon atoms to which they are bonded, a monocyclic or bicyclic azacycloalkane group. The invention also relates to the pharmaceutically acceptable salts thereof, to the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof.
CA2184916C Use of fibroblast growth factors to stimulate bone growth The present invention provides therapeutic compositions for the prevention and treatment of pathological conditions involving bone and dental tissue. The present invention also provides a method to promote bone repair and/or growth for the treatment of pathological conditions involving bone tissue, for example, osteoporosis, Paget's disease, osteopetrosis, and periodontal disease and fracture repair, and healing of bone defects by administering FGF-I to an animal or human in need of said treatment.
WO2006079217A1 Treatment of degenerative diseases with the x-linked inhibitor of apoptosis Methods and compositions comprising vectors expressing XIAP or XIAP protein preparations for the treatment of degenerative disorders including retinal degeneration, skeletal muscular atrophy, spmal muscular atrophy (SMA), spmobulbar muscular atrophy (SBMA), amyolateral sclerosis (ALS), muscular dystrophy, Parkinson's disease, cardiac injury, and liver disease, and for the reduction of cell apoptosis during transplantation of cells are provided.
EP1511489A1 New pharmaceutical compositions containing flibanserin polymorph a The invention relates to oral pharmaceutical compositions containing flibanserin polymorph A , methods for the preparation thereof and use thereof as a medicament.
WO2006018807A1 Crystalline forms of cefdinir The invention relates to processes for the preparation of crystalline polymorphic forms of cefdinir of formula I. More particularly, it relates to the preparation of crystalline polymorphic forms of cefdinir designated as Forms B and C. The invention also relates to pharmaceutical compositions that include the polymorphic forms B and C, and the use of the compositions for treating bacterial infections.
US7119098 Antitumor agents; osteoporosis; antiarthritic agents; oral diseases The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the ανβ3 and/or the ανβ5 integrin without significantly antagonizing the IIb/IIIa integrin.
CN101606994A Plaster for treating bone rheumatism The invention discloses a plaster for treating bone rheumatism, which is prepared from nux vomica, folium artemisiae argyi, cassia twig, notopterygium root, rhubarb, radix clematidis, stir-fry radix aconiti agrestis, pawpaw, stephania tetrandra, lycopodium clavatum, herba siegesbeckiae, achyranthes, suberect spatholobus stem, frankincense, myrrh, eucommia bark, teasel root, radix angelicae tuhuo, parasitic loranthus, earthworm, Chinese ephedra, cinnamon, muskiness and borneol. The plaster is convenient to use, has no toxic side effect, quick effect and difficult recrudescence after healing and also has 96 percent of effective rate and 80 percent of cure rate on treating the bone rheumatism.
US7993829 HPRP4s modifiers of the p53 pathway and methods of use Human hPRP4 genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of hPRP4 are provided.
CN102000226A Medicine for treating hemiplegy The invention provides a medicine for treating hemiplegy, which is characterized by being prepared through the following steps of: taking 9g of whole angelica, 12g of membranous milkvetch root, 3g of obscured homalomena rhizome, 9g of large-leaved gentian, 9g of parasitic loranthus, 3g of lumbricus, 6g of root of red-rooted salvia, 5g of Kadsura Pepper Stem, 6g of suberect spatholobus stem, 9g of dragon's teeth, 12g of shell of abalone, 6g of magnetic stone and 12g of Indian bread with pine; carrying out decoction 2 times with one dosage of the drug per day; and separately taking the medicine in the morning and in the evening, wherein 30 days is taken as a course of treatment and the medicine is bound to be continuously taken for 2-3 courses of treatment. The treatment effect of the medicine is optimal and the clinical curative rate is up to 90 percent.
CA2612161A1 Use of non-steroidal progesterone receptor modulators The present invention relates to the use of non-steroidal progesterone receptor modulators of the general formula (I) for the therapy and prophylaxis of gynaecological disorders and of hormone-dependent tumours, and for use for female fertility control and for hormone replacement therapy.
CN102614500A Biological plant alcohol relieving and liver protecting capsule The invention relates to a biological plant alcohol relieving and liver protecting capsule, which is used for protecting the gastric mucosa and the liver before and after drinking, can accelerate the decomposition of in vivo alcohol, and has the functions of alcohol relieving, liver protecting, lipid lowering, and stomach protecting. The capsule has the advantages of reaching of liver and stomach protecting functions before drinking, obvious alcohol relieving effect, alcohol capacity increase, lipid lowering, no side effect, toxin release, immunity enhancement, and convenient carrying.
EP1797887A1 Drug for diminishing increase of neutral fat in blood after meal and food containing the same The present invention herein provides an agent or a food for inhibiting a postprandial increase in blood neutral fat level. The agent or food comprises, as an effective component, a water-soluble and hardly digestible starch decomposed product having a content of hardly digestible components of at least 35% by mass. The water-soluble and hardly digestible starch decomposed product can be ingested separately or simultaneous with a high fat-content meal.
US20120071455 6-substituted demethyl-estradiol derivatives as selective er-beta agonists Disclosed herein are 6-substituted 13-demethyl-estradiol derivatives as selective ERβ agonists. Also disclosed is a method for treating pain by administering these 6-substituted 13-demethyl-estradiol derivatives.
WO2007089934A3 Methods of treating alcoholism and alcohol related disorders using combination drug therapy and swellable polymers The current invention provides methods of treating alcohol related disorders by providing a sustained release oral drug dosage form comprising a plurality of solid state drugs i.e., baclofen and naltrexone, dispersed in a solid state unitary matrix formed from a combination of swellable polymers. The combination of swellable polymers in a single oral drug dosage form is beneficial in terms of release rate control for combination therapies.
CN101229159A Medicine for treating infectious diarrhea and peptic ulcer, preparing method and applications thereof The invention which provides a drug curing infectious diarrhea and peptic ulcer comprises the effective components of 1 to 48 percent of rifaximin and 52 to 99 percent of convergent protective agent. The drug of the invention can prevent the synthesis of bacteria RNA, kill the bacteria RNA and can also neutralize the gastric acid to avoid the abscission of gastrointestinal mucosa caused by the infectious diarrhea so as to protect the gastrointestinal mucosa and accelerate the body rehabilitation. The invention improves the efficacy, reduces the toxicity and shortens the course of treatment on the present technical base and also provides a preparation method and application of the drug of the invention.
WO2005110438A2 Methods and products related to the intracellular delivery of polysaccharides The invention relates, in part, to methods and compositions for the intracellular delivery of polysaccharides. In particular, the methods and compositions relate to the intracellular delivery of glycosaminoglycans, such as heparin. The invention in other aspects relates to the use of glycosaminoglycans for the treatment of proliferative disorders, such as cancer. The invention is still other aspects relates to improving cell viability. The invention also relates to the delivery of polysaccharides while avoiding unwanted effects of the polysaccharides. For example, heparin can be delivered while avoiding its anticoagulant effects.
US20050042318 Controlling hormone sensitive diseases; solvent extraction of hops, filtration, desolventizing Novel extracts from hop with an increased content of prenylated chalcones and flavones, methods for producing the same, pharmaceutical preparations comprising such extracts of hop and use of these extracts of hop for the prophylaxis and treatment of pathological conditions caused by oestrogen deficiency or by dysregulations to sex-hormone-related metabolism are described.
CA2415966C Tetrahydro-heterocycloazepinyl pyrimidine derivatives The invention relates to compounds of the general formula (I) wherein HET and R1 to R12 have the significances as defined in the specification, as well as their phamaceutically acceptable salts. The invention further relates to medicaments containing such compounds and a process for the preparation of such compounds. The compounds of formula (I) are group (I) mGluR antagonists and are therefore useful for the control or prevention of acute and/or chronic neurological disorders.
US20080306144 Hydroxybenzyl or hydroxypyranonemethyl esters as tyrosinase inhibitors Method for the preparation of ester compounds for use as skin brightening agents and compositions for brightening skin containing the ester compounds.
WO2012046771A1 Cycloalkane compound The inventors have intensively studied on compounds that have Aβ42 production inhibitory activity and have found that a compound (I) of the present invention, wherein a carboxylic acid or a tetrazole group is bonded to a cycloalkane moiety via a linker and an amine is bonded to the cycloalkane moiety directly or via a linker, or a pharmaceutically acceptable salt of the compound strongly inhibits the production of Aβ42. In addition, the inventors have found that these compounds have excellent γ secretase function modulating action, and thus have completed the present invention.
EP2344496A1 Amides of diazabicyclooctanes and uses thereof The present invention relates to compounds of the following formulae I and II that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS). Formula (I ), Formula (Il)
CN103446176A Chlorhexidine and oligochitosan-containing pharmaceutical composition and applications thereof The invention relates to a chlorhexidine and oligochitosan-containing pharmaceutical composition, wherein the mass proportion of the chlorhexidine to oligochitosan is (0.1-1):1, the chlorhexidine comprises chlorhexidine acetate, chlorhexidine gluconate, chlorhexidine hydrochloride or chlorhexidine citrate, and the molecular weight of the oligochitosan is less than 5,000. The invention further relates to an application of the pharmaceutical composition in preparing a skin or object surface sanitizer, an application of the pharmaceutical composition in preparing an air-atomizing sanitizer, an application of the pharmaceutical composition in preparing an oral cavity sanitizer, an application of the pharmaceutical composition in preparing a vaginal irrigation solution, or an application of the pharmaceutical composition in preparing vaginal gels. According to the chlorhexidine and oligochitosan-containing pharmaceutical composition, the oligochitosan plays a role in obviously improving the antibacterial action of the chlorhexidine.
EP0842268B1 Methods and compositions for identifying morphogen analogs Disclosed herein are methods and compositions for identifying morphogen analogs. Preferred methods rest on the use of test cells comprising DNA defining a morphogen-responsive transcription activating element operatively associated with a reporter gene. In certain embodiments, the methods involve an osteogenic protein 1 (OP-1) responsive transcription activating element. Substances that activate the OP-1 responsive transcription activating element are considered herein likely to be useful for reproducing in vivo effects of morphogens such as OP-1.
DE102007041473A1 Use of glycyrrhetinic acid and/or glycyrrhizin for manufacturing cosmetic or dermatological preparations to strengthen the natural skin tanning, treat skin and hair and reduce wrinkles Use of glycyrrhetinic acid and/or glycyrrhizin (I) for manufacturing cosmetic or dermatological preparations to strengthen the natural skin tanning, is claimed. - ACTIVITY : Dermatological. - MECHANISM OF ACTION : None given.
CN102164909A Pyrine or pyrazine derivatives for treating HCV Compounds having the formula I wherein R1, R2a, R2b, R2c, R3, Y and p are as defined herein and C2-C3 is a single or double bond are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
CN103142532A Ginkgolide osmotic pump tablet and preparation method thereof The invention provides a ginkgolide osmotic pump tablet and a preparation method thereof. The ginkgolide osmotic pump tablet provided by the invention is a double-layer tablet composed of a drug-containing layer and a push layer, and is coated, wherein the drug-containing layer comprises drug release holes. The ginkgolide osmotic pump tablet uses ginkgolide at effective positions of the ginkgo biloba extract as an active component, and a total amount of ginkgolide A, ginkgolide B, ginkgolide Cand bilobalide is not less than 70 %. According to the invention, by combining a solid dispersion solubilising technique and an osmotic pump tablets control-release technology, the ginkgolide is firstly prepared into the solid dispersion, and then further prepared into the ginkgolide osmotic pump tablet on a basis of improving solubility of poorly soluble components, thereby realizing synchronous slow release of complex components in the ginkgolide, reducing drug administration times and improving patient compliance.
CN101756936A Oral antiviral medicament The invention relates to an oral antiviral medicament, namely an oral cidofovir preparation, in particular to a soft capsule comprising the cidofovir and a preparation method thereof.
US20060052315 Cb 1/cb 2 receptor ligands and their use in the treatment of pain Compounds of formula (I) or pharmaceutically acceptable salts thereof wherein Ar 1?, Ar 2?, R 1?, R
WO2014152564A1 Methods of acute restoration of vascular compliance Disclosed herein is a compound for use in a composition applied to a blood vessel, wherein the compound softens and/or disrupts the crystalline matrix of calcified plaque, as well as acutely restoring the vascular compliance at the treatment site of the blood vessel, while maintaining luminal gain during angioplasty. Methods of treatment comprising applying the disclosed composition are also disclosed. Plaque-softening compounds are also disclosed.
EP1397170B1 Safety shield system for prefilled syringes A medical device (10) is provided which includes a shield system (14) and a syringe (12) which is coupled to the shield system. The shield system includes a syringe holder (26) and a shield (28) which is slidably coupled to the holder. A spring (30) resiliently urges the shield from a retracted position to an extended position. Stop members (48, 52) are provided on the holder and shield for maintaining the shield in the retracted position. The syringe is slidably coupled to the holder, and extends within the shield. Axial movement of the syringe with respect to the holder causes disengagement of the stop members, allowing the spring to move the shield to the extended position. Detends (58, 59) are provided on the holder for maintaining the shield in the extended position.
US20120195850 Use of polymer d-lactic acid (pdla) or equivalents thereof to inhibit growth of cancer cells and diagnose cancers The invention provides method for sequestering or trapping L-lactate in or near a tumor cell comprising contacting an isolated polymer of D-lactic acid (PDLA) or an equivalent, derivative or analog thereof with the tumor cell so that the PDLA binds L-lactate in or near the cell and thereby sequestering or trapping L-lactate in or near the tumor cells.
CN102552797A Preparation method of quick-release Xingnaojing lozenge The invention relates to a preparation method of a quick-release Xingnaojing lozenge. The preparation method of the quick-release Xingnaojing lozenge comprises the following steps of according to a Xingnaojing prescription amount, carrying out water boiling extraction of active components of cape jasmine fruits, carrying out freeze drying to obtain cape jasmine fruit dry extract, extracting turmeric root-tuber volatile oil by a steam distillation method, carrying out clathration of the turmeric root-tuber volatile oil with beta-cyclodextrin to obtain a turmeric root-tuber volatile oil clathrate, carrying out ethanol reflux extraction of musk active ingredients, dissolving borneol into musk extract obtained by the previous step, carrying out clathration with beta-cyclodextrin to obtain a clathrate of the borneol and the musk active ingredients, respectively crushing the cape jasmine fruit dry extract, the turmeric root-tuber volatile oil clathrate and the clathrate of the borneol and the musk active ingredients, mixing, adding appropriate amounts of auxiliary materials into the mixture, and carrying out processing to obtain the quick-release Xingnaojing lozenge.
US20090099246 Veliparib crystal structure; an anticancer PARP inhibitor 2-((R)-2-Methylpyrrolidin-2-yl)- I H-benzimidazole-4-carboxamide Crystalline Form 2, ways to make it, compositions comprising it and made using it, and methods of treating patients having disease using it are disclosed.
CA2850558A1 Beta-lactam compounds for treating diabetes Compositions and methods comprising ampicillin or salts and derivative thereof for the treatment of delaying the onset of type I diabetes are provided.
US20110268798 Orally disntegrating tablets for the treatment of pain An orally disintegrating tablet comprising acetylsalicylic acid, acetaminophen and caffeine and one or more pharmaceutically acceptable excipients.
CN1615883A Compound medicine for treating hepatitis B virus and controlling HBV virus duplication The present invention relates to medicine technology, and is especially a kind compound medicine for treating hepatitis B and inhibiting HBV duplication. The compound medicine contains ebselen, propagermanium and lamivudine, which complement and synergize mutually to treat hepatitis B. The present invention has the functions of protecting liver cell, regulating immunity, restoring liver function, resisting virus and preventing liver fibrillatioin.
CN1634077A Orally disintegrating tablet of levonogestrel and its preparing process The invention provides an orally disintegrating tablet of levonogestrel and its preparing process, wherein the preparation is prepared by using Levonorgestrel as the medicament, using lactose, mannitol, low substituted methylcellulose propylene glycol ether, magnesium stearate, 95% ethanol, menthol as raw material by a finite proportion, wherein wet method granulation and pelleting are carried out, the prepared orally disintegrating tablet has a hardness of 1.0-3.5 kg, it can be disintegrated within 1 minute, the disintegrated powder can pass through 24 mesh Levonorgestrel disintegrating tablet.
CN101130515A Substituted-1H- indoles compound, method for preparing the same, application and pharmaceutical composition of the same The invention discloses a substituted-1H-indole compound with general formula as formula (I) and medically acceptable salt, solvent complex or hydrate, wherein Ar, R1, R2, n, X and Rx in the formula is defined as instruction; the compound has better prevention and cure action for experimental inflammation; the compound is dual inhibitor of epoxy oxygenase and 5-lipoxidas, which displays strong effective inhibitor for 5-lipoxidas; therefore the compound can be developed into safe non-steroidal anti-inflammatory agent to treat asthma, allergy and other immune disease and cardiovascular disease and/or prevention drug. The invention also provides the making method of the compound and its drug composition.
WO2012166463A2 Aminooxazole inhibitors of cyclin dependent kinases Oxazoie derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
WO2008052044A2 Use of derivatives of propofol for treating diseases associated with oxidative stress Methods of treating diseases associated with oxidative stress such as metabolic diseases, cardiovascular diseases, neurological diseases, liver diseases, and pulmonary diseases in a patient comprising orally administering a therapeutically effective amount of forms of propofol that provide a high oral bioavailability of propofol are disclosed.
CN101837008A Ointment for curing intractable dermatosis of animals The invention discloses an ointment for curing intractable dermatosis of animals. The ointment is characterized in that the ointment comprises the following components: 600 to 800g of sulfur powder, 200 to 400 IU of penicillin and 50 to 150g of ivermectin. The invention provides the ointment for curing the intractable dermatosis of animals, which has good curative effects on the disease through the proportion of the medicinal components such as the sulfur powder, the penicillin, the ivermectin and the like. The ointment has the advantages of simple components and low cost, and is suitable for popularization and use in breeding farmers.
US20110160236 Treating Vascular Events with Statins by Inhibiting PAR-1 and PAR-4 The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.
WO2012149454A3 Tolerogenic synthetic nanocarriers coupled to cd1d-restricted antigens and methods of use Disclosed are synthetic nanocarrier compositions, and related methods, comprising CD1d-restricted antigens and immunosuppressants that provide tolerogenic immune responses.
WO2014142116A1 Ceramide-like function imparting agent Provided are: a ceramide-like function imparting agent which imparts a function similar to that of a ceramide; a skin barrier function reinforcing agent; a moisturizing agent; and an external preparation for the skin. A ceramide-like function imparting agent which contains, as an active ingredient, a succinic acid diamide derivative represented by formula (1). (In the formula, each of R1 and R2 independently represents a hydroxyalkyl group having 1-6 carbon atoms; and R3 represents a -CH2CH2CH2CH2-R4 group or a -CH2CH=CHCH2-R4 group (wherein R4 represents an alkyl group having 8-26 carbon atoms).)
WO2012171793A1 Selective cns delivery of mifepristone (ru486) to modulate the timing of the spontaneous lh surge during follicular stimulation cycles The present invention relates to a new pharmaceutical product containing an antiprogestin molecule, such as mifepristone (RU486), administered by the nasal route and to be used to modulate the timing of the spontaneous LH surge as part of foliicular stimulation cycles intended for Assisted Reproductive Technology (ART). In particular, it details the route of administration and the dosages that ensure effective delay of the LH surge without incurring in the antifo!liculogenetic effects of the antiprogestinic. It also details the overall treatment method as resulting from the use of the new drug product.
US20110311625 Solid dosage forms of fenofibrate An improved solid dosage form of fenofibrate which exhibits improved dissolution properties leading to increased bioavailability of fenofibrate. A novel core-shell approach to the composition is provided as well as a process for the preparation of the improved solid dosage forms.
WO2007058995A1 Manually actuated contactless card A manually actuated contactless card includes at least one manual actuator and a memory having at least one record of confidential information. The manually actuated contactless card provides the at least one record of confidential information to a reader when the manually actuated contactless card is energized by the reader provided that at least one of the manual actuators is simultaneously actuated.
WO2013172999A1 Pharmaceutical compositions for the delivery of substantially water-insoluble drugs The subject invention relates to compositions and methods useful for the in vivo delivery of substantially water-insoluble drugs, like taxol. The use of specific composition and preparation conditions enables the reproducible production of unusually water -soluble formulation, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a re-dispersible dry powder comprising nanoparticles of drug. The innovation is also based on the fact that complementary partner is also an active drug but may have a different mode action with respect to primary molecule of the hybrid drug. The complementary molecule has multiple properties like antioxidant, antimicrobial, anti-inflammatory, anti-allergic, cox-2 inhibitors, etc. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable.
WO2007026254A3 Benzodiazepine derivatives , their preparation and the therapeutic use thereof The invention relates to benzodiazepine derivatives having PDE2 inhibitory activities, as well as therapeutic methods by administering said compounds, in particular for treating various diseases of the central or peripheral nervous system. It further deals with pharmaceutical compositions comprising said compounds and methods for preparing said compounds.
US20110151025 Compositions Comprising N-Halogenated or N,N-Dihalogenated Amine for Treatment and Prophylaxis of Bronchopulmonary Infections Disclosed herein are methods and compositions for the treatment or prophylaxis, in a mammal, of bronchopulmonary infections, obstructive pulmonary disease, cystic fibrosis, and ventilator-associated infections. The methods and compositions include a therapeutically effective amount of one or more N-halogenated or N,N-dihalogenated amines, and their analogues, derivatives, or pharmaceutically acceptable salts and esters.
CN102114033A Fragrant preparation for preventing sleepiness and preparation method thereof The invention discloses a fragrant preparation for preventing sleepiness and the preparation method thereof. The fragrant preparation is prepared from the following components according to parts by weight: 0.1-0.5 parts of methyl salicylate, 40-60 parts of menthol, 10-20 parts of borneol, 20-30 parts of camphor, 40-50 parts of diphenyl ether, 1-3 parts of sodium thiosulfate, and 120-160 parts of 2wt% chlorine dioxide solution. The preparation method comprises the following steps: (1) preparing 2wt% chlorine dioxide solution; and (2) homogenously mixing methyl salicylate, menthol, borneol, camphor and diphenyl ether, adding into the 2wt% chlorine dioxide solution, stirring, and standing for 30 h; and adding sodium thiosulfate to remove odor. The fragrant preparation disclosed by the invention can be used for preventing sleepiness, and has the advantages of simple preparation process, good efficacy, very low dose, no toxic and adverse effects and no skin irritation.
WO2013084210A9 Amorphous form of sitagliptin salts The present invention claims amorphous solid state forms of sitagliptin salts, processes for their preparation, and pharmaceutical compositions thereof. As salt forming anions are claimed: The maleate, fumarate, besylate, mesylate and succinate. (Formula (I))
WO2007024599A3 Comination of a hypnotic agent and r(+)-alpha-(2,3-dimethoxy-phenyl)-1-[2-(4-fluorophenl)ethyl]-4-piperidinemethanol and therapeutic application thereof The invention concerns the combination of a short-acting hypnotic agent and R-(+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol (Compound A) or its prodrug of the Formula II wherein R is C1-C20 alkyl or a pharmaceutically acceptable salt thereof. The combination of this invention is useful in treating a variety of sleep disorders.
CN1931308A Dermatosis treating medicine The present invention discloses Baifuling cream as medicine for treating dermatosis, and the medicine is prepared with zinc oxide, aloe, dexamethasone, DDS, fish liver oil and vaseline in certain weight proportion, and through grinding and mixing. Baifuling cream of the present invention has simple preparation process, low cost, high healing effect on herpes and allergic dermatosis and short treating period.
CN103102284A Preparation of 4-trifluoromethyl-2, 6-dinitrobenzene salicylaldoxime derivative and its application in anticancer therapeutic drugs The invention relates to a 4-trifluoromethyl-2, 6-dinitrobenzene salicylaldoxime derivative, which is characterized by having the following general formula. In the structural formula, R1 can be hydrogen, 5-chlorine, 3, 5-dichloro, 5-bromo, and 3, 5-dibromo, and R2 can be hydrogen, 2-fluoro, 2-chloro, and 2, 4-dichloro. The 4-trifluoromethyl-2, 6-dinitrobenzene salicylaldoxime derivative provided in the invention can resist tubulin polymerization and inhibit the proliferation of MCF7, HepG2, A549 cells. Therefore, the salicylaldoxime compound provided in the invention can serve as a potential antitumor drug. The invention discloses its preparation method.
WO2009139972A3 Site specific fluorescence marking and contrast marker for same A contrast marker for indicating a presence of a target cell in an environment comprises a fluorophore, an NMP, and a short spacer and a long spacer linking the fluorophore to the NMP. The short spacer holds the fluorophore at a quenching distance from the NMP and the long spacer holds the fluorophore at a fluorescence enhancing distance from the NMP. The short spacer is configured to be cleaved by a molecule characterizing the target cells.
US7531544 Xanthine phosphodiesterase V inhibitors A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:
CN103027892A Penfluridol self-micro-emulsifying nano composition and preparation method thereof The invention discloses a penfluridol self-micro-emulsifying nano composition and a preparation method thereof. The penfluridol self-micro-emulsifying nano composition comprises the following components in percentage by weight: 0.2-19.0 percent of penfluridol, 1.0-10.0 percent of oil phase, 5.0-55.0 percent of surfactant and 0.0-25.0 percent of cosurfactant. The self-micro-emulsifying nano technology is combined with penfluridol, the medicine can be self-emulsified into micro-emulsion particles of 1mu m in vivo, such as oral soft capsules, hard capsules, oral liquid and granules; or the medicine exists in a sterile solution form of a transdermal delivery system in vitro, such as preparation of ointment, gel patch and the like. According to the prepared self-micro-emulsifying nano composition, the adverse effect of the medicine is reduced, the absorption rate of the medicine is improved, the bioavailability of the medicine is improved, the curative effect of the medicine is enhanced, and the administration compliance of a patient is improved.
WO2008048577A1 Methods of using 4-phenylaminoquinolines as topical non-steroidal antiinflammatory compounds A skin disorder, a disorder associated with pain, fever, or inflammation, a proliferative disorder, or an ocular disorder is treated by topically administering a pharmaceutically acceptable formulation containing a therapeutically effective amount of a 4-phenylaminoquinoline compound.
WO2013056079A1 High affinity beta lactamase inhibitors Inhibitors of beta lactamases and their use in treating bacterial infections are dicslosed.
CN101797223A Huperzine A preparations for eyes and application thereof The invention relates to Huperzine A preparations for eyes and application thereof. The Huperzine A preparations for the eyes can be applied to preparing medicaments for preventing and treating glaucoma, increase of intraocular pressure and eye problems concomitant with retinal ganglion cell injury; and the preparations for the eyes are Huperzine A eye drops and a Huperzine A in-situ-gel for eyes. The invention has the advantages that: the Huperzine A eye drops and the Huperzine A in-situ-gel for eyes are successfully developed, and the two formulations are convenient for ophthalmic patients to use. The Huperzine A in-situ-gel for eyes is liquid with good fluidity in vitro; when the Huperzine A in-situ-gel is dropped into eyes, the formulation is easily controlled accurately and the use is convenient; and after the Huperzine A in-situ-gel is dropped into eyes, the Huperzine A in-situ-gel can be uniformly spread to form a gel, stays in the eyes for a long time, is not easily lost to be absorbed by the whole body, can maintain local effective medicament concentration so as to improve bioavalability, has low toxin and acrimony and good biocompatibility, is an effective medicament for treating the glaucoma, and has wide development prospect.
CN101569627B Folic acid acceptor mediated molecular targeted photosensitizer and preparation method thereof A molecular targeted photosensitizer and a preparation method thereof are disclosed. The molecular targeted photosensitizer consists of folic acid porphyrin, R1, R2 and R3 in the molecular structural formula of folic acid porphyrin are independently hydroxyl, straight-chain or branched-chain hydrocarbon, n in the molecular structural formula ranges from 1 to 20. The preparation method is as follows: alkylation reaction is carried out on monohydric porphyrin and dihalohydrocarbon to generate halogen porphyrin, and then Gabriel reaction is carried out with phthalimide potassium to generate amideporphyrin which is hydrolyzed by hydrazine to obtain primary amine porphyrin; finally, amination reaction is carried out on primary amine porphyrin and folic acid to obtain the folic acid porphyrin.The raw materials used by the preparation method of the invention are stable and accessible, the reaction condition is mild, the yield is high, the generated reactant has good targeted therapy to tumor cell, partial photosensitizer in vitro photodynamic antitumor activity result shows strong effect, thus being suitable for tumor targeted photodynamic therapy and having good clinical application value.
US8632823 Treatment of infected tissues with hypochlorous acid Super-oxidized water based on hypochlorous acid, such as is obtained by the electrochemical treatment of a saline solution, may be used in the treatment of leg ulcers or other open wounds. Preferably, the pH of the super-oxidized water is in a range of 4 to 7, and the water has a redox potential of >950 mV. Medicaments based on the super-oxidized water may be in liquid or gel form. The super-oxidized water is able to control the microbial population within the wound and at the same time permit cell proliferation.
US20080319061 Process for the Preparation of an Oxaliplatin Preparation The present invention relates to an improved process for the preparation of oxaliplatin, the obtained oxaliplatin preparation and its use in cancer therapy.
CN103637997A Duloxetine hydrochloride medicament composition, enteric sustained release preparation and preparation method thereof The invention provides a duloxetine hydrochloride medicament composition, an enteric sustained release preparation and a preparation method thereof. The enteric sustained release preparation comprises the following components in parts by weight: 5-40 parts of duloxetine hydrochloride, 35-65 parts of sodium alginate, 5-20 parts of calcium salt, 15-35 parts of filler and 0.5-20 parts of lubricant. The medicament composition and the enteric sustained release preparation provided by the invention are hardly released under the gastric acid condition, so that a main medicine is prevented from being damaged in a stomach, no functional sustained release coating is needed to control medicine release, no enteric sustained release material is needed, only high-velocity sodium alginate and other medical auxiliaries are used, the enteric effect is achieved by adjusting the ratio, meanwhile the sustained release function is achieved, the medicine is effectively prevented from being damaged by the gastric acid environment, and the stability of the medicament inside a body in the absorption process is maintained.
US20120141553 Biocompatible polymer fibres for neuroimplants The present invention relates to a neuroimplant. The neuroimplant comprises biocompatible polymer fibres; the polymer fibres are grouped in a parallel arrangement, and the group of fibres is flexible. The present invention also relates to the use of the neuroimplant to facilitate the repair of damaged brain tissue.
US8426400 β-lactamyl phenylalanine, cysteine, and serine vasopressin antagonists Substituted 2-(azetidin-2-on-1-yl)alkoxyalkylalkanoic acids and 2-(azetidin-2-on-1-yl)arylalkylalkanoic acids, and analogs and derivatives thereof are described. Methods for using the described compounds, and pharmaceutical compositions thereof, to treat disease states responsive to antagonism of one or more vasopressin receptors are also described.
WO2005087713A1 Amide compound, pharmaceutical composition and rxr function control agent Disclosed is an amide compound having high activity as an RXR ligand which is free of side effects. Also disclosed are an RXR function control agent composed of such an amide compound, an RXR/PPAR heterodimer function control agent composed of such an amide compound, and a pharmaceutical composition containing such an amide compound. Specifically disclosed is a compound represented by the general formula (1) below or a salt thereof. (In the formula (1), R1-R4, Ar, V, W and Z are as specifically defined in claims and the description.)
WO2013024474A8 Polymorphs of preladenant The present invention provides novel crystalline forms of preladenant, pharmaceutical compositions comprising same, methods for their preparation and use thereof in treating a neurodegenerative disease, especially Parkinson's Disease (PD).
US20130018065 Processes for the preparation of key intermediate for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-methanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.
US7423063 calcium salt is calcium trifluoroacetate; to prepare medicaments with cytotoxic and antitumoral activity Calcium salts, in particular calcium trifluoroacetate, are added to medicaments to provide cytotoxic and antitumoral activity. The medicaments can be administered to cancer patients as part of a method of treating a cancer patient. The medicaments can also be applied to a tumor to treat the tumor. The medicaments may be administered or applied orally or parenterally.
US8080263 Dispersion for pulmonary delivery of a bioactive agent Stabilized dispersions are provided for the delivery of a bioactive agent. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a liquid fluorochemical. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments the stabilized dispersions may be directly administered to the lung of a patient using an endotracheal tube or bronchoscope.
US20130035389 Methods for treating myelodysplastic syndrome with ezatiostat This invention relates to methods, assays, devices and systems for identifying patients having a myelodysplastic syndrome for treatment with ezatiostat or a salt thereof, or evaluating the patient's response possibility to the treatment by measuring and evaluating the patient's gene expression profile. This invention also relates to methods of treating myelodysplastic syndromes.
EP1792998A2 An unusual retrotransposon from the yeast Candida albicans TCa2 is a Tyl/copia retrotransposon from the pathogenic yeast Candida albicans. In contrast to other retrotransposons it can appear as an abundant, extrachromosomal double-stranded DNA molecule, called pCal. The invention relates to the isolation and characterisation of TCa2 and pCal together with its uses for inducing random mutagenesis in a genome, as a component of a transposable element and of an expression vector.
CN103479625A Application of Fluevirosines A in preparation of blood sugar reducing medicines The invention discloses an application of Fluevirosines A in the preparation of blood sugar reducing medicines. The application proves that the Fluevirosines A has a substantial anti-diabetic effect, is a compound having a clear chemical structure, has a brand new skeleton type, has a strong diabetic controlling activity, has protruding substantive characteristics, and substantially improves the diabetic treatment.
US20080233122 Complementarity determining regions; immunoglobulins; cell line, host cells; transgenic animals, plants In accordance with the present invention, there are provided fully human monoclonal antibodies against human cytotoxic T-lymphocyte antigen 4 (CTLA-4). Nucelotide sequences encoding and amino acid sequences comprising heavy and light chain immunoglobulin molecules, particularly contiguous heavy and light chain sequences spanning the complementarity determining regions (CDRs), specifically from within FR1 and/or CDR1 through CDR3 and/or within FR4, are provided. Further provided are antibodies having similar binding properties and antibodies (or other antagonists) having similar functionality as antibodies disclosed herein.
US7105558 Gastrin and cholecystokinin receptor lignads (iv) Compounds of the formula (I) or (II) and their pharmaceutically acceptable salts are ligands at gastrin and/or chole-cystokinin receptors n is from 1 to 4; R4 is C1 to C15 hydrocarbyl wherein up to two C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; Z is —(NR5)a—CO—(NR6)b-(wherein a is 0 or 1, b is 0 or 1, and R5 and R6 are independently selected from H, Me, Et, Pr, Bn), —CO—NR5—CH2—CO—NR6—, —CO—O—, —CH2—CH2—, —CH═CH—, CH2—NR6— or a bond; Q is R7V, or(a) wherein R7 is —CH2—; —CH2—; or(b) R7 and R6, together with the nitrogen atom to which R6 is attached, form a piperidine or pyrrolidine ring which is substituted by V; V is —CO—NH—SO2-Ph, —SO2—NH—CO-Ph, CH2OH, or a group of the formula —R8U, (wherein U is —COOH, tetrazolyl, —CONHOH— or —SO3H; and R8 is a bond; C1 to C6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamino; —O—(C1 to C3 alkylene)-; —SO2NR9—CHR10—; —CO—NR9—CHR10—, R9 and R10 being independently selected from H and methyl; or —NH—(CO)c—CH2—, c being 0 or 1); m is 1 or 2; q is from 0 to 2, with the proviso that q is 1 or 2 when Z is a bond); Compositions comprising a compound of formula (I) or (II) are also described.
CA2220080C Method for making quinolone carboxylic acids or naphthyridine carboxylic acids in free base form The present invention provides a method of making quinolone carboxylic acids or naphthyridine carboxylic acids in free base form, the method comprising dissolving a quinolone carboxylic acid salt or naphthyridine carboxylic acid salt in a solvent system to form a solution;combining the solution containing the quinolone carboxylic acid salt or naphthyridine carboxylic acid salt with a calcium salt in an amount in the range of about 0.01 % to about 5.0 % by weight of the quinolone carboxylic acid salt or naphthyridine carboxylic acid salt and a base, the combination resulting in the formation of a precipitate; and collecting the precipitate. Also provided is a solid bulk pharmaceutical chemical composition comprising 7-(3-amino-1-pyrrolidinyl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or 7-(3-S-(2-S-aminopropionylamino)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid; and calcium in an amount in the range of 0.001 % to about 1.0 % by weight of the 7-(3-amino-1-pyrrolidinyl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or 7-[3-S-(2-S-aminopropionylamino) pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid.
WO2007009691A3 Combination of substituted pyrazolines and anti -addictive agent The present invention relates to an active substance combination comprising at least one substituted pyrazoline compound and at least one anti-addictive compound, a medicament comprising said active substance combination, a pharmaceutical formulation comprising said active substance combination and the use of said active substance combination for the manufacture of a medicament.
EP1999131A2 Bicyclo-pyrazoles active as kinase inhibitors A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.
US20100168149 Camptothecin Analogue Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them Compound of formula (I): wherein: R1, R2, R3, R4, R5, R80, R90, R81, R91, Alk and G are as defined in the description. Medicinal products containing the same which are useful in the treatment of cancer diseases.
US20100093794 Use of a Compound in Obtaining Cytoskeleton Blockage and Cell Elongation A use of a compound in obtaining cytoskeleton and cell elongation is disclosed, the compound is 7-chloro-6-piperidin-1-yl-quinoline-5,8-dione with a chemical formula of C14H13CIN2O2, is designated as PT-262. The PT-262 can induce cell elongation by stabilization of the F-actin and induction of the abnormal actin polymerization in cancer cells, further, the PT-262 possesses antitumor activity and can block survival pathway of the cancer cells, resulting in cancer cells apoptosis, and the PT-262 can induce growth arrest and inhibition of cell cycle. PT-262 stabilizes cancer cells cytoskeleton that results in an irreversible cell elongation, decreases the levels of cyclin B1 and phospho-cdc2 proteins, and inhibits the survival signal pathway of Ras-ERK proteins. The PT-262 also inhibits the mitochondrial membrane potential and induces the caspase-3 activation and apoptosis in the cancer cells.
CN101072558A Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1 ):wherein the symbols have the meanings given in the specification. and tautomers, stereoisomers and N -oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N -oxides.
CN1736485A Use of vanillin receptor agonist in preparation of product for resisting Alzheimer disease The invention relates to the use of vanillic aldehyde receptor activator in preparing products against Alzheimer's disease, wherein the vanillic aldehyde receptor activator comprises vanillic aldehyde and its derivative, capsaicin analogue and derivatives.
WO2008022784A3 Long-lasting absorption of flavonoids The present invention relates to methods for a long-term and sustained release of flavonoids, in particular rhamnose-containing flavonoids, and for prolonging the uptake of said flavonoids in the gastro-intestinal tract. It further relates to compositions comprising said flavonoid and α-rhamnosidase. It also encompasses compositions comprising hesperidin and hesperetin-7-glucoside.
CN101559044A Clopidogrel hydrosulfate enteric coated tablet and preparation thereof The invention relates to a clopidogrel hydrosulfate enteric coated tablet and the preparation thereof. The clopidogrel hydrosulfate enteric coated tablet comprises enteric coated granules containing clopidogrel hydrosulfate or the mixture of the clopidogrel hydrosulfate and other accessories, and main component of coated liquid is water solution containing methacrylic acid copolymer. An isolating membrane is coated on active raw materials or the active raw materials and other accessories. The clopidogrel hydrosulfate enteric coated granules can inhibit the disintegration and the release of the clopidogrel hydrosulfate under the condition that the pH value is lower than 5, and can rapidly disintegrate and release the clopidogrel hydrosulfate under the condition that the pH value is higher than 6.
US20110318422 Targeted active agent delivery system based on calcium phosphate nanoparticles Calcium phosphate nanoparticle active agent conjugates are described. Specifically, anticancer agent conjugates are prepared which are suitable for targeted active agent delivery to tumor cells and lymphatics for the treatment of cancer and the treatment or prevention of cancer metastasis.
EP1126782B1 Method for improved imaging and photodynamic therapy The present invention is directed to an apparatus and method of imaging and treatment using at least one photodynamic therapy ('PDT') agent. The method includes administering a photoactive agent to a patient (56), imaging the patient to locate the diseased tissue or tumors (54) in the patient using an imaging device (52) such as CAT scan or MRI, and treating the imaged diseased tissue with light (60) sufficient to photo-activate the agent in the tissue.
EP1021464B1 Cellular receptor for hiv-1 vpr essential for g2/m phase transition of the cell cycle The present invention is directed to substantially pure Human Vpr Interacting Protein (hVIP), and fragments thereof. Also disclosed are isolated nucleic acid molecules that encode hVIP, or a fragment thereof; nucleic acid probes and primers directed to nucleic acid molecules that encode hVIP, or a fragment thereof; oligonucleotide molecules that consist of a nucleotide sequence complementary to a portion of the nucleotide sequence that encodes hVIP; vectors comprising nucleic acid molecules encoding hVIP; recombinant expression vectors that comprise nucleic acid sequences that encode hVIP; host cells that comprise recombinant expression vectors which include nucleic acid sequences that encode hVIP; genetic therapy vectors comprising nucleic acid molecules encoding hVIP; isolated antibody which binds to an epitope on hVIP; pharmaceutical compositions comprising a pharmaceutically acceptable carrier and nucleic acid molecules complementary to a portion of hVIP; methods of making hVIP; and methods of inhibiting expression of hVIP oligonucleotides complementary to a portion of the nucleotide sequence that encodes hVIP.
US20080194658 N-(4-{[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]amino}phenyl)acetamide; treating high serum levels of total cholesterol, low density lipoprotein and triglycerides Methods of treating high serum levels of total cholesterol, low density lipoprotein and triglycerides in a mammal by administering therapeutically effective doses of N-(4-{[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]amino}phenyl)acetamide or a salt thereof such as a hydrochloride or hydrobromide salt.
EP2404599A1 Neuroprotective compounds The invention describes the use of (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl-1-naphthalenyl propanoate derivatives, optionally mono- or di-methylated at the carbon in the alpha position of propanoic acid, of formula (I), where R is CH3CH2CO-, (CH3)2CHCO- or (CH3)3CCO-, its hydroxy acid forms and the pharmaceutically acceptable salts of said hydroxy acids, as neuroprotective compounds potentially useful for the prevention and/or treatment of neurodegenerative diseases, or of diseases associated with an unwanted oxidation or of age-associated pathological processes, or of epilepsy, epileptic seizures or convulsions.
WO2012136349A1 Tapentadol for preventing chronification of pain The invention relates to tapentadol for use in the treatment of pain in a subject suffering from pain chronification and/or for use in the treatment or the prevention of pain chronification. The invention also relates to tapentadol for use in the treatment or prevention of migraine.
CN101947209A Divalproex sodium pellets and preparation method thereof The invention relates to divalproex sodium pellets and a preparation method thereof. The divalproex sodium pellets consist of divalproex sodium, filling agent, adhesive, lubricating agent and pH adjustor. The preparation method mainly comprises that the divalproex sodium and the adhesive are prepared into the medicinal pellets by an extrusion rounding method. The preparation method has the advantage that the preparation process is simple and feasible; the prepared divalproex sodium pellets can be processed into enteric coated pellets and can be further processed into multiple oral preparations such as capsules, suspension and the like; the bioavailability of the divalproex sodium is effectively improved; the dissolution in acid is ensured to meet the requirement of pharmacopeia for enteric coated preparations at the same time of reducing the use of enteric coating by a novel method using the pH adjustor, and the gastrointestinal stimulation is reduced; and the divalproex sodium pellets solve the problems of low bioavailability and high intestinal stimulation of the conventional enteric coated tablets.
US8367738 Smooth muscle contraction inhibitors An emulsion comprising L-Menthol, a fat or oil and a surfactant wherein oil particles have an average diameter of 100 nm or less inhibits a content reduction attributed to, for example, evaporation of L-menthol, enhances a light transmission through liquid and is stable despite long-term storage. Thus, the emulsion can be appropriately used in the temporary inhibition of contraction of gastrointestinal tract for, for example, observation of gastrointestinal tract by an endoscope. This emulsion can be obtained by heating an oil-in-water type emulsion comprising L-menthol, a fat or oil and a surfactant at 60° C. or higher.
CN102675206A Preparation method of novel acetylcholinesterase inhibitor, and activity thereof The invention relates to the field of medicine, and specifically relates to a preparation method of a cyano (or nitro) carbamidine (imidazole) derivative, and investigates acetylcholinesterase inhibitory activity of the derivative. The invention provides a compound shown in structural formula (I), wherein B, A, M, N, W, Y and X are defined in specification. The invention also relates to applications of compounds shown in structural formula (I) as acetylcholinesterase inhibitor.
CN102924554A C-3,11,12,20-tetrasubstituted C-21 steroid derivative and its pharmaceutical composition and use in medicine The invention provides a C-3,11,12,20-tetrasubstituted C-21 steroid derivative shown in the general formula I and its pharmaceutical salt and glycoside, and also provides a pharmaceutical composition containing the C-3,11,12,20-tetrasubstituted C-21 steroid derivative as an active ingredient and a use of the C-3,11,12,20-tetrasubstituted C-21 steroid derivative in preparation of a medicine for treating epilepsy. In the general formula I, R1, R2 and R3 respectively represent a ketonic group, a hydroxyl group, a substituted acyl ester group, an amino-group or a substituted acylamino group; R4 represents a ketonic group, a hydroxyl group, a substituted acyl ester group, an amino-group, a substituted acylamino group, or a glycosyl group; and R5, R6 and R7 respectively represent hydrogen, a hydroxyl group, a substituted acyl ester group, an amino-group or a substituted acylamino group.
EP1800684A1 Novel alkyl phospholipid derivatives and uses thereof The present invention provides novel alkyl phospholipid derivatives that are useful for treating various diseases including tumors and/or pathophysiological conditions in mammals, preferably humans, that are caused by microorganisms, in particular fungi, protozoa, bacteria and/or viruses. Such alkyl phospholipids can be employed as single drugs or in the course of combination therapies, in particular for the treatment of leishmaniasis, trypanosomiasis and/or malaria.
CN102000097A Bunge auriculate root C21 total steroidal glycoside degradation product and antitumor effect thereof The invention relates to the field of natural medicines, in particular to a bunge auriculate root C21 total steroidal glycoside degradation product, which is characterized by being prepared by the following steps of: degrading dry powder of the C21 total steroidal glycoside of bunge auriculate root in the presence of acid or alkali, regulating the pH to be 7, extracting by using an organic solvent, and recovering the organic solvent. The bunge auriculate root C21 total steroidal glycoside degradation product has strong antitumor effect.
WO2008078762A1 Novel n-(2-aminophenyl)benzamide derivative having an urea structure Disclosed are: a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of the pharmacological activity of the derivative. A compound represented by the general formula (1) or a salt thereof has an activity of changing the morphology of a trabecular cell and therefore is effective for the prevention and/or treatment of a disease associated with an ocular tension. In the formula, R1 and R2 independently represents a hydrogen atom, a lower alkyl group or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group or the like; R4 and R5 independently represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group or the like; l and m independently represent a number of 0, 1, 2 or the like.
US20090148451 Therapeutic anti-cytomegalovirus compounds The present invention provides synthetic compounds, antibodies that recognize and bind to these compounds, polynucleotides that encode these compounds, and immune effector cells raised in response to presentation of these epitopes. The invention further provides methods for inducing an immune response and administering immunotherapy to a subject by delivering the compositions of the invention.
US20080132508 compound that inhibits glycosphingolipid synthesis; includes PPMP, PDMP, or NB-DGJ or any derivative or analog thereof or any derivative of ceramide that inhibits glycosphingolipid metabolism Diabetic retinopathy is a debilitating complication of diabetes and a leading cause of vision loss, however the fundamental mechanisms contributing to vision loss remain undefined. Several novel observations are described: 1) diabetic retinas demonstrate decreased total ceramide levels; 2) with a concomitant increase in glucosylceramides; 3) which mediates decreased insulin receptor signaling and; 4) cell death in vitro and in vivo. Inhibition of this dysfunctional glycosphingolipid metabolism restores insulin sensitivity. Moreover, elevation in diglycerides and reduction in concentrations of phosphatidic acid or ceramide-1-phosphate also contribute to diabetic complications and insulin resistance. The mechanism responsible for dysfunctional lipid metabolism in diabetic tissues involves reduced caveloin-1-expression within structured membrane microdomains and suggest another target for molecular and pharmacological intervention. Preferred embodiments describe pharmacological and molecular systems and methods to therapeutically alter dysfunctional lipid metabolism and restore selective insulin-dependent kinase cascades as well as membrane integrity.
WO2010117014A1 Triazine derivative Disclosed is a novel triazine derivative represented by formula (I), which has FAAH inhibitory activity and is useful as an analgesic. (In the formula, Ar1 represents an optionally substituted aromatic heterocyclic group, and Ar2 represents a phenyl group which may be substituted by one or more halogen atoms.)
WO2008119685A2 Oxazolidine and morpholine carboxamide derivatives as p2x7 modulators The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
CN101967152A New methylenedioxy xanthone compound and anti-tumor effect thereof The invention relates to a new methylenedioxy xanthone compound and anti-tumor effect thereof. The invention also relates to application of the compound in preparation of a medicament, particularly preparation of an anti-tumor medicament.
US7276517 Heterocyclic amide derivatives as inhibitors of glycogen phosphorylase Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof, possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
US20070258996 Synergistic combination of three or more of sequestering agents, carbohydrates, terpenes or terpenoids, amines, plant-derived oils, sulfonates, phenols, fatty acids, dibenzofuran derivatives, organo isothiocyanates, quaternary ammonium compounds, peroxides or macrolide polyenes; antiobiotic resistance An antimicrobial composition, including a synergistic combination of three or more potentiating agents as an active ingredient. Each of the three or more potentiating agents may be selected from the following types of compounds: sequestering agents, carbohydrates, terpenes, terpenoids, peptides, alkaloids, plant-derived oils, dyes and stains, sulfonates, phenols, esters, fatty acids, and dibenzofuran derivatives. At least two of the three or more potentiating agents are not of the same type of compound. The antimicrobial composition may have strong antimicrobial efficacy in control of microorganisms having resistance to currently used antimicrobials.
CN102961325A Cream containing fenticonazole nitrate and preparation method thereof The invention discloses cream containing fenticonazole nitrate and a preparation method thereof. The cream is used for treating infections caused by dermatomycosis, tinea corporis, dermatophyte, saccharomycetes and other fungi, is processed by adopting a scientific and reasonable production process, has definite functions and controllable quality and is safe to take. The medicine composition provided by the invention can be prepared by using a simple method and conventional equipment.
US20090105254 Vhr protein tyrosine phosphatase inhibitors, compositions and methods of use Disclosed herein are Vaccinia H1-related (VHR) protein tyrosine phosphatase (PTP) inhibitors that provide a method for treating cancer.
US20110150766 Transdermal patch with fatal overdose protection A transdermal patch having a top region containing an antagonist followed by a bottom region containing an agonist, whereby the bottommost end of the bottom region is secured to the skin of the patient for delivering a prescribed dosage of agonist to the patient over a predetermined period of time, the antagonist will be released by migrating or moving from the top region through the bottom region to the patient to prevent overdose. Visual indicators are provided in the patch for changing color to separately indicate the operation of the patch, delivery of prescribed dosage, and/or overdosage.
EP1723105A1 Bicyclic substituted indole-derivative steroid hormone nuclear receptor modulators The present invention provides a compound of the formula: Formula (I); or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, hypertension, and atherosclerosis, comprising administering to a patient in thereof an effective amount of a compound of Formula I. X-16125
CN102048741A Antiallergic medicament and application thereof The invention relates to a medicinal compound which prevents and treats diseases such as inflammation, allergy, infection and the like and a preparation method and application thereof. The invention also discloses a compound which comprises an active ingredient I serving as adrenomimetic cortical hormone or pharmaceutically acceptable salt of the compound and a medicinal composition consisting of one or more of pharmaceutically acceptable carriers, excipients or diluents.
US20100196493 Method for producing stable powder compositions The invention relates to the use of at least one viscous compound, the viscosity of which is greater than 5 Pa·s−1, to substantially prevent the degradation of a substance sensitive to temperatures of 20° C. to 100° C. and/or pressures of 106 to 107 Pa and/or a relative humidity of 60% to 100%, contained in a powder composition, the powder composition containing particles including: a core containing the sensitive substance and at least one viscous compound as impregnating agent for the sensitive substance and a coating for the core, which contains at least one viscous compound as sticking agent.
EP1100481B1 Pharmaceutical formulations comprising beclomethasone dipropionate for the treatment of inflammatory bowel disease The invention relates to pharmaceutical formulations for the treatment of inflammatory bowel disease containing as active ingredient Beclomethasone dipropionate. A first aspect concerns a formulation in the form of stable and ready-to-use enema characterized in that the homogeneity of the active ingredient at low concentration (0.05 %) and fluidity of the suspension is optimal for promoting its retrograde progression and homogeneous distribution. A second aspect concerns gastro-resistant modified-release tablets whose composition has been optimized in order to control the release of the active ingredient in fluids at basic pH and low ionic strength.
WO2009081837A1 Pharmaceutical composition for ameliorating lower urinary tract symptom Disclosed is a pharmaceutical composition useful as a pharmaceutical composition for ameliorating lower urinary tract symptom. Specifically disclosed is a pharmaceutical composition comprising, as active ingredients, (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2- phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof and (R)-5-(2-{[(2- (2-ethoxyphenoxy)ethyl)amino]propyl}-2-methoxybenzene-1- sulfonamide or a pharmaceutical acceptable salt thereof particularly for ameliorating lower urinary tract symptom, more specifically for ameliorating lower urinary tract symptom associated with prostatomegaly.
CN101778632A Remedy or preventive for integration dysfunction syndrome It is intended to provide a preventive or remedy for integration dysfunction syndrome by which integration dysfunction syndrome, in particular, positive symptoms thereof, can be treated without inducing information-processing disorder relating to cognition disorder, i.e., one of the syndromes of integration dysfunction syndrome. Thus, a preventive or remedy for integration dysfunction syndrome, which comprises as the active ingredient a compound having a specific morphinane skeleton typified by the following compound 1 or a pharmacologically acceptable acid addition salt thereof, is provided.
CA2156078C New imidazopyridines The invention relates to novel compounds of the formula I(see formula I) wherein R0 is methyl or hydroxymethyl, R1 and R2 are 1-4C alkyl, R3 is 1-4C alkoxy and A is O or NH, and the therapeutic use thereof.
US20100330021 Substituted (thiazol-2-yl)-amide or sulfonamide as glycokinase activators useful in the treatment of type 2 diabetes Compounds of the formula R—NH-Q (I) provide pharmacological agents which are glucokinase activators and thus may be employed for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for prevention and treatment of impaired glucose tolerance, Type 2 diabetes and obesity.
CN103467426A Quercetin hydrocarbylation derivative and preparation method and application thereof The invention provides a quercetin hydrocarbylation derivative which is characterized in that in a general formula (1), R1, R2, R3 and R4 are respectively and independently selected from H, (CH2)3CH3, CH2CH=CHPh, CH2CH=CH(CH3)CH3, and CH2CH=CH(CH3)CH2CH2CH=CH(CH3)CH3, and the R1, the R2, the R3 and the R4 are not all Hs.
CN103211781A Etoposide soft capsule The invention relates to an etoposide soft capsule, and aims to provide a novel etoposide soft capsule that can overcome the defects of etoposide, improve the bioavailability of etoposide, have rapid absorption and take rapid effect. The applicant unexpectedly find that combined application of polyethylene glycol and citric acid can greatly improve the stability and dissolving speed of etoposide, thus completing the invention.
CN101343272A Carbpenem compound containing cyclohexane The invention belongs to the medical technique field, particularly relating to hydrates containing carbapenem compounds of cyclohexane, acceptable salt thereof in pharmacy, easily hydrolysable ester thereof, isomers thereof, hydrate thereof, as well as ester or salt thereof as shown in a general formula (1): wherein, R<1>, R<2>, R<3>, R<4>, R<5> and X are defined in the specification; and the invention also relates to a preparation method of the compounds, a medical composition containing the compounds, and applications of the compounds in preparing medicines for curing and/or preventing infectious diseases.
US6867299 Inosine monophosphate dehydrogenase (IMPDH); use as immunosuppressants, anticancer agents and antiviral agents Disclosed are compounds of the general formula which are oxamide derivatives and inhibitors of the enzyme inosine monophosphate dehydrogenase (IMPDH).
CN102772599A Lumbago plaster The invention discloses a lumbago plaster for dredging channels and activating collaterals. The lumbago plaster is prepared from the following raw materials in parts by weight: 12-17 parts of radix angelicae pubescentis, 8-12 parts of radix bupleuri, 12-16 parts of semen vaccariae, 12-17 parts of radix aucklandiae, 1-4 parts of whole centipede, 12-17 parts of Chinese polyphaga, 1-3 parts of seman sinapis albae, 1-3 parts of lysimachia trientaloides hemsl, 1-3 parts of small centipeda herb, 3-6 parts of mulberry twig, 3-6 parts of herba taxilli, 3-6 parts of herba aristolochiae, 7-9 parts of caulis lonicerae, 8-12 parts of arisaema consanguineum schott, 8-12 parts of camphora, 3-6 parts of radix aconiti and 12-17 parts of rhizoma ligustici chuanxiong. The lumbago plaster disclosed by the invention has the effects of dredging channels and activating collaterals and dissipating cold and removing dampness, is suitable for various kinds of lumbago, has a good curative effect, takes an effect quickly, and is convenient to use.
US20130064865 Therapy to reduce extravasation damage A method of treating a patient who has extravasation of blood from an intravascular compartment to an extravascular compartment. An agent is administered to the patient which mitigates a harmful effect of break-down products of blood at an extravascular site, resulting in the patient having reduced morbidity and mortality. The morbidity and mortality of the patient is further reduced by concomitant administration of a suspension of submicron protein spheres having a molecular weight of ranging from 780 billion Daltons to less than 0.8 billion Daltons.
WO2004062671A3 Pde4 inhibitors for the treatment of neoplasms of lymphoid cells The invention relates to the use of certain PDE4 inhibitors alone or in combination with one or more differentiation inducing agents and/or an agent effective in raising intracellular concentrations of cAMP or a stable analogue of cAMP in the preparation of pharmaceutical compositions for the treatment of neoplasms of lymphoid cells.
US8546366 Method for inhibition of tumor cell growth using (22R)-5α-lanosta-8,24-dien-3β,15α,21-triol In this patent, we isolated a novel compound from fruiting body of Antrodia cinnamomea, namely, (22R)-5α-lanosta-8,24-dien-3β,15α,21-triol. This compound possesses preferential cytotoxicity against human leukemia, pancreatic cancer, esophageal cancer, hepatoma, and cervical cancer cells.
EP1725549A1 Pentafluorosulfanyl compounds, their manufacture and use as pharmaceutical agents Objects of the present invention are the compounds of formula I-A (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
WO2013095169A1 Crystalline minocycline thermo-resistant obtained by recrystallization with carbon dioxide The present invention relates to a novel form of minocycline chlorohydrate characterized in that- it is crystalline and it presents characteristic powder X-ray diffraction pattern and infrared spectrum. This new polymorph constitutes the most stable form of minocycline with a melting point much higher than that of other known crystalline forms of minocycline. The process of production of this new minocycline polymorphic form consists in the dissolution of carbon dioxide in solutions or suspensions of minocycline chlorohydrate with organic solvents, under certain conditions of pressure and temperature. The present invention places minocycline in the restrict group of antibiotics with a melting temperature higher than the sterilization temperature, which enhances new applications and allows the optimization of production at industrial
CN1846704A Eye protecting capsule and dripping agent preparing process The eye protecting capsule and dripping agent are compounded with vitamin A powder, taurine, glucose injection and distilled water. It is used to prevent eye diseases, nurse eyes, delay senility, raise eyesight, diminish inflammation, detocate, relieve pain and eliminate fatigue. It has simple recipe, determined curative effect, no side effect, convenient use, no pollution, simple preparation process and low cost.
CN103126978A Preparing method for ambroxol hydrochloride injection The invention discloses a preparing method for ambroxol hydrochloride injection. The preparing method for the ambroxol hydrochloride injection includes the following steps that each 2ml of the injection comprises, by weight, 15 mg of ambroxol hydrochloride, 4.0 mg of disodium hydrogen phosphate, 1.16 mg of citric acid and 14 mg-16 mg of sodium chloride; water for injection is cooled to be below 30 DEG C; the disodium hydrogen phosphate and the citric acid are added into the water for injection to be dissolved; a prescribed dosage of ambroxol hydrochloride raw medicine is added to be dissolved; the sodium chloride is added to adjust solution to be isotonic; the solution is filtered through a 0.22-micrometer millipore filter; and the solution is filled and sterilized after high purity nitrogen gas is let in. The preparing method for the ambroxol hydrochloride injection is simple in process and stable in product quality.
EP2785712A1 Homomultivalent and heteromultivalent inhibitors of prostate specific membrane antigen (pmsa) and uses thereof The present invention provides bivalent and multivalent ligands with a view to improving the affinity and pharmacokinetic properties of a urea class of PSMA inhibitors. The compounds and their synthesis can be generalized to multivalent compounds of other target antigens. Because they present multiple copies of the pharmacophore, multivalent ligands can bind to receptors with high avidity and affinity, thereby serving as powerful inhibitors. The modular multivalent scaffolds of the present invention, in one or more embodiments, contains a lysine-based (α-, ε-) dialkyne residue for incorporating two or more antigen binding moieties, such as PSMA binding Lys-Glu urea moieties, exploiting click chemistry and one or more additional lysine residues for subsequent modification with an imaging and/or therapeutic nuclides or a cytotoxic ligands for tumor cell killing.
US20070299135 Compositions for Use in Surgery A method is provided for treating a subject in need of medication as an adjunct to elective surgery, comprising administration of a ketogenic material sufficient to produce a physiologically acceptable ketosis in the patient. Preferably the surgery is selected from the groups consisting of removal or section of tumours, removal of redundant organs such as lymph nodes and appendix, open heart surgery, cosmetic surgery, joint and bone surgery.
CN102988700A Preparation method of tinea pedis soaking agent The invention discloses a preparation method of a tinea pedis soaking agent. The method comprises the following steps of: (1) dissolving 0.05-0.3% of pyridine ammonium bromine, 10-30% of garlic oil, 10-20% of pepper extracting solution and 0.1-2% of metronidazole in an appropriate amount of sterile water, and evenly stirring; (2) mixing 10-30% of garlic oil and 2-10% of medical glycerine, and then evenly stirring; (3) mixing the mixtures obtained in the steps (1) and (2); and (4) adding sterile water and complementing till 100%, and evenly stirring to obtain the finished product. The tinea pedis soaking agent prepared by the invention can effectively and thoroughly kill pathogenic bacteria.
CN102070699A Trihydroxy-substituted pentacyclic triterpene compounds and preparation method and application thereof The invention discloses a group of trihydroxy-substituted pentacyclic triterpene compounds and a preparation method and application thereof. The general formula of the compounds is shown in the structural formula I, wherein R1 and R2 are selected from hydrogen or methyl, R3 is selected from any one of -COOH, -CH2OH, -CHO, -COOR1, -CONH2, -CONHR1 and -CONR1R2, R1 and R2 are selected from one of alkyl containing 1-8 carbon atoms, substituted or unsubstituted phenyl and substituted or unsubstituted alkylphenyl, R2 and R1 are identical or different, the hydroxide radical substitution configurations of C1, C2 and C3 are alpha-configurations or beta-configurations, and the compound 1 alpha,2 alpha-dyhydroxy oleanolic acid and 1 alpha,2 alpha-dihydroxy ursolic acid are excluded. The invention provides a group of compounds with novel structures and a synthesis method thereof. The compounds and the salts thereof have obvious protection effects of liver injury, and the synthesis method can be used for preparing liver-protecting medicines; and the synthesis method has mild reaction conditions, no special apparatuses are needed, the operation is simple and practical and the synthesis method is easy to enlarge scale and achieve industrial production.
WO2008101052A8 Compositions and methods for treating, reducing, ameliorating, or preventing infections of the ear or upper respiratory tract Compositions for treating, reducing, ameliorating, or preventing infection of an ear or upper respiratory tract comprise a fluroquinolone having Formula I, II, or UI. Methods for treating, reducing, ameliorating, or preventing such infection use such compositions. Such compositions and methods can be effective against certain antibiotic-resistant microbial pathogens found in such infection.
US20110190351 Benzoimidazole Derivatives and Glycogen Synthase Kinase-3 Beta Inhibitors Containing the Same Benzoimidazole Derivatives are provided. The compounds of the present invention are useful for Glycogen Synthase Kinase-3 Beta Inhibitors.
US20080004258 such as [2-(3,4-Dichloro-phenoxy)-5-(4-morpholin-4-yl-but-1-ynyl)-benzyl]-methyl-amine, used as H3 receptor and/or serotonin transporter modulators useful in the treatment of cognitive, sleep and psychological disorders Certain substituted butyl and butynyl benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
CN101422452A Use of rosmarinic acid and plant extract containing rosmarinic acid The invention discloses a compound rosmarinic acid shown in formula I; the chemical name thereof is: (R(E)) Alpha-((3-(3, 4 dihydroxyphenyl)-1-oxo-2-propenyl)oxo)-3, 4-dioxy-benzene monoprop. Or, the invention discloses the application of a plant extract thereof containing the compound in preparing a digestion-related enzyme activity inhibitor as well as preparing medicaments, drinks, foods and healthcare products for inhibiting the raising of the sugar content of blood, preventing and controlling or curing diabetes or adiposity, or losing weight, beautifying and shaping a body. The application of the invention expands a new application field for the compound and simultaneously provides a new approach for preventing, controlling and curing diseases in the fields, and for health care.
US20110142796 Fused Pyridine, Pyrimidine and Triazine Compounds as Cell Cycle Inhibitors Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
US20100331274 Antiaging Chirally-Correct Mitoprotectant Amino Acid and Peptide Complexes This invention relates to certain chirally-correct mitoprotectant phosphorylated heterocyclic agents [formula (I)], which are useful for the treatment of dermatological disorders that include challenged skin from cancer, diabetes, radiation treatments, chemotherapy, and sun-burn; mitochondrial dysfunction; age spots; acne, loss of cellular antioxidants; skin changes associated with aging including collagen loss, loss of skin pliability, loss of skin suppleness, skin wrinkles and fine lines, oxidation, damage from radiation, damage from free radicals, and damage from UV; dry skin; xerosis; ichthyosis; dandruff; brownish spots; keratoses; melasma; lentigines; liver spots; skin pigmentation including pigmented spots, dark circles under the eyes, darkened skin, and blemishes; oily skin; warts; eczema; pruritic skin; psoriasis; inflammatory dermatoses; topical inflammation; disturbed keratinization; scalp dryness; skin depigmentation, and combinations thereof;
CN103751195A Method for treating oral ulcer The invention discloses a method for treating oral ulcer. Oral ulcer has the symptoms of eating and drinking difficulty and intolerable pain. Some oral ulcer self-treatment methods are conducive to oral ulcer treatment. The method comprises that vitamin C and vitamin B2 are ground into powder; a small amount of the powder is applied to small-area aphtha; and exudates on the surface of large-area aphtha are lightly scraped and the large-area aphtha is coated with the powder.
WO2011102577A1 Novel use for scopolin and derivatives thereof The present invention relates to a novel use for the compound of Chemical formula 1 in order to produce drugs or foods for the prevention or treatment of obesity, fatty liver, diabetes, metabolic syndrome or the like, and to a composition for the prevention or treatment of obesity, fatty liver, diabetes, metabolic syndrome or the like which contains the compound of Chemical formula 1 as an active ingredient, and also to a method for the prevention or treatment of obesity, fatty liver, diabetes, metabolic syndrome or the like comprising the administration of the compound of Chemical formula 1 to a mammal in a therapeutically effective dose. According to the present invention, the compound of Chemical formula 1 has been confirmed to suppress the differentiation of adipocytes, to reduce body weight and the amount of visceral fat, to reduce concentrations of cholesterol, triglycerides, free fatty acids and glucose which are associated with fatty liver and diabetes and the like and to reduce the fatty component in liver tissue, to suppress gene expression associated with obesity in visceral fatty tissue, and to increase the amount of expression of UCP1 and UCP3 which are UCP (uncoupling protein) genes involved in thermogenesis. The compound of Chemical formula 1 can be used to advantage in order to prevent or treat obesity, fatty liver, diabetes, metabolic syndrome and the like since, unlike the obesity treating agents based on synthetic drugs currently in use, it is based on a natural substance and hence entails a very low risk of side effects and, additionally, it exhibits its pharmacological effects by regulating the expression of genes associated with obesity rather than exhibiting pharmacological effects by acting on enzymes or the nervous system.
CN103536929A Preparation method of HPMC (Hydroxyl Propyl Methyl Cellulose) liquor The invention discloses a preparation method of HPMC (Hydroxyl Propyl Methyl Cellulose) liquor. The method comprises the following steps: adding 1-2 parts of HPMC by weight into 50-100 parts of absolute ethyl alcohol; stirring to wet and disperse HPMC in the ethyl alcohol; gradually adding 5-10 parts of pure water; stirring; and standing for 10-30 minutes to prepare the HPMC liquor. According to the preparation process disclosed by the invention, the ethyl alcohol is used as a solvent to effectively reduce oxidation and damage of products which are sensitive to water and are easy to be oxidized and damaged by water, so that the final product has relatively high stability and good purity. The preparation method is convenient for industrialized production.
US20120077867 Compositions And Methods For Treating Pancreatic Cancer The present invention provides a method of treating pancreatic cancer by inhibiting the activity cyclin D1 activity in tumor cells. The invention is based on the finding that cyclin D1 shRNA molecules are capable of attenuating tumor growth and interfering with tumor angiogenesis.
EP1320710B1 Drying method for selectively removing volatile components from wet coatings Method of selectively removing volatile components from a composition, comprising coating the composition onto a first substrate surface of a substrate (38), wherein the composition comprises a nonresident volatile component and a resident volatile component. The method further includes positioning at least a portion of the coated substrate (36) between a condensing surface (32) having a condensing surface temperature (Tc) and a heating surface (34) having a heating surface temperature (TH) that is greater than the condensing surface temperature, wherein the condensing surface (32) is in a spaced apart, confronting relationship to the coated surface (44) of the substrate (38) and wherein the heated surface (34) is in thermal contact with a second substrate surface (42) opposite the first substrate surface. In the method, the heated surface temperature (TH) and the condensing surface temperature (Tc) are such that the positioning step causes the nonresident volatile component to be selectively removed from the portion of the coated substrate. The method is suitable for forming transdermal drug delivery compositions (36).
CN101921810B Method for preparing xylitol and L-arabinose mixed crystal from xylose mother liquid The invention provides a method for preparing a xylitol and L-arabinose mixed crystal from xylose mother liquid and relates to a method for preparing rare sugar alcohols in the biotechnology field. The invention describes a method for preparing a xylitol and L-arabinose mixed crystal from xylose mother liquid by a biological method. The method comprises the following steps of: inoculating yeast (Candida sp)X828 CGMCC No.3691 which cannot use L-arabinose as a unique carbon source to a xylose mother liquid culture medium to ferment; consuming glucose and galactose in the xylose mother liquid; reducing the xylose to obtain xylitol so as to obtain xylitol and L-arabinose-containing fermentation liquid; and concentrating, desalting, reconcentrating and crystallizing the fermentation liquid to obtain the xylitol and L-arabinose mixed crystal. In the method, an additional value of the xylose mother liquid can be increased; and the xylitol and L-arabinose mixed crystal can be directly used for preparing a product which comprises the L-arabinose and the xylitol at the same time.
WO2011075784A1 Compounds, preparations and uses thereof The present invention provides novel compounds of the Formula (I), pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.
CN101390833A Anti-cancer slow-release formulation loaded with carmustine and synergist thereof Disclosed is an anticancer sustainable-release agent, which contains the combination of carmustine and carmustine synergist. The anticancer sustainable-release agent is injection and implantation agent; the sustainable-release injection contains sustainable-release microspheres which contain effective anticancer ingredients and sustainable-release auxiliary material, and special solvent which contains suspending agent; the viscosity of injection is 50cp-1000cp(20 DEG C-30 DEG C); the suspending agent is selected from one or the combination of the followings, sodium carboxymethyl cellulose, mannitol, sorbitol, tween 80. The sustained-release auxiliary material is selected from copolymer of the combination of the followings, polylactic acid, ethylene vinyl acetate copolymer, polifeprosan, FAD: sebacic acid copolymer, polyglycolic acid and glycolic acid; the sustained-release auxiliary material is high-molecular polymer with biological capability and degradable absorption; the effective anticancer ingredients can be sustainably released on the local part of tumor during the degradable absorption process of the sustained-release auxiliary material so that the systemic toxic reaction caused by the sustained-release agent is obviously reduced; meanwhile, the effective medicine concentration is maintained in local part of the tumor.
CN102887880A Dibenzofuran derivatives, and preparation method and application thereof The invention provides dibenzofuran derivatives. The compounds have excellent cholinesterase inhabitation activity and mild A beta fibration inhibition activity. The invention also provides a preparation method for the compounds and application of the compounds to application of the compounds to preparation of medicines for treating neurodegenerative diseases. The structural formula of the compounds is shown in the specifications.
CN202568929U Tablet capsules containing rosiglitazone solid preparation and metformin solid preparation The utility model relates to oral hard capsules, in particular to tablet capsules filled with metformin tablets and rosiglitazone tablets. The tablet capsules comprise capsules and tablets disposed in the same. Each capsule consists of an upper capsule and a lower capsule. Each capsule is filled with at least one tablet with metformin active ingredient and at least one tablet with rosiglitazone active ingredient. The tablet capsules contain the metformin tablets and rosiglitazone tablets, various active ingredients in the capsules do not contact with one another, and accordingly the tablet capsules better in stability and convenient to process are obtained.
US20070281931 Pharmaceutical Composition Containing a P2x7 Receptor Antagonist and Methotrexate The invention provides a pharmaceutical composition, pharmaceutical product or kit comprising a first active ingredient which is a P2X7 receptor antagonist, and a second active ingredient which is N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamic acid (methotrexate) or a pharmaceutically acceptable derivative thereof, for use in the treatment of inflammatory disorders.
CN102641289A Tinea removing beverage removing skin caring liquid The invention relates to tinea removing beverage removing skin caring liquid, which resolves the technical problem by adopting the technical scheme that the skin caring liquid comprises 1000ml of purified water, 0.3g to 0.5g of borneol, 6g to 16g of sodium benzoate, 50ml to 60ml of ethanol, 6g to 10g of citric acid, 50ml to 80ml of glycerin, 6g to 28g of borax, 0.5g of vitamin C, 6g to 10g of sodium hydrogensulfite, 10.5g of vitamin B, 1g to 3g of potassium sorbate, 60.5g of vitamin B6, 1g to 2g of ethylparaben and 1g to 3g of cellulose glycolate. The tinea removing beverage removing skin caring liquid has the advantages of being simple in preparation, easy to achieve and capable of effectively treating various tinea, getting effect instantly and simultaneously having remarkable whitening and beverage removing effects.
US6878522 Methods for the identification of compounds useful for the treatment of disease states mediated by prostaglandin D2 The present invention relates to the discovery that PDG2 is the nautral ligand for orphan receptor CRTH2, which interaction, it will now immediately be recognized, is important in the development of valuable pharmaceuticals. The present invention is therefore related to methods for screening for therapeutic compounds useful in the treatment of PGD2-related disorders such as allergy, asthma and inflammation. Appropriate assay methodology is also disclosed.
CN101337956A Scutellarein carbamate derivates, preparation method and application thereof The invention relates to a novel scutellarin aglycon 4 (1)-position carbamate derivant (1), a preparation method and the application thereof. A pharmacological experiment proves that the compounds have obvious inhibitory activity of acetylcholinesterase and have protective effect with different degrees on PC12 cell trauma induced by H2O2, so the compounds can be used for preparing the drugs for treating neurodegenerative diseases such as vascular dementia, AD (presenile dementia), etc.
US20090156554 N-[1-(3-dimethylamino-4-formyl-phenyl)-3-pyridin-3-yl-4,5-dihydro-1H-pyrazolo[4,3-g]benzothiazol-7-yl]-acetamide; phosphatidylinositol-3-kinases (PI3-kinases) inhibitor; cell growth, differentiation and intracellular transport processes; antiproliferative, antiinflammatory agent; autoimmune diseases New compounds of formula 1 are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.
US20130018007 Modified Saponins for the Treatment of Fungal Infections Methods of treating a fungal infection in a subject, the method comprising administering to the subject a modified saponin.
WO2008053331A1 Alpha-substituted omega-3 lipids that are activators or modulators of the peroxisome proliferators-activated receptor (ppar). Omega-3 lipid compounds of the general formula (I): wherein R1 and R2 are the same or different and may be selected from a group of substitu- ents consisting of a hydrogen atom, a hydroxy group, an alkyl group, a halogen atom, an alkoxy group, an acyloxy group, an acyl group, an alkenyl group, an al- kynyl group, an aryl group, an alkylthio group, an alkoxycarbonyl group, a car- boxy group, an alkylsulfmyl group, an alkylsulfonyl group, an amino group, and an alkylamino group; - X represents a carboxylic acid or a derivative thereof, a carboxylate, a carboxylic anhydride or a carboxamide; and - Y is a C16 to C22 alkene with two or more double bonds, having E and/or Z configuration, are disclosed. Also disclosed are pharmaceutical compositions and lipid compositions comprising such compounds, and to such compounds for use as medicaments in particular for the treatment of cardiovascular and metabolic diseases.
CN102911222A Extraction method of aucubin and application of aucubin The invention relates to an extraction method of aucubin and an application of the aucubin. The method comprises the simple steps of crushing plantain, soaking in alcohol overnight, conducting ultrasonic extraction, merging, recovering, concentrating and centrifuging an extracting solution, obtaining supernate, adopting macroporous resin and eluting an alcohol solution, conducting thin-layer chromatography detection, collecting and concentrating fraction at a target point, conducting silicagel column chromatography on a concentrate, and then collecting and concentrating the fraction at the target point, repeating the silicagel column chromatography to obtain macrocrystalline, purifying a crude product through high performance liquid chromatography, collecting target components, freezing and drying, and finally obtaining white amorphous powder. The substance extracted from the plantain by the method is the aucubin. The aucubin can be used for treating and preventing diabetes mellitus and concurrent encephalopathy of the diabetes mellitus, the occurrence and development mechanisms of the diabetes mellitus and complications of the diabetes mellitus are further deeply studied, and new-generation drugs for resisting the diabetes mellitus and the complications of the diabetes mellitus can be developed.
WO2008049123A3 2,4-pyrimidinediamine derivatives as inhibitors of jak kinases for the treatment of autoimmune diseases The invention encompasses compounds having formula (I) and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.
CN101670110A Hydrogel controlled by hydrogen bond and pi-pi accumulation biswitch and preparation and application thereof The invention relates to a PMAA and PAA base hydrogel which has a sequential lamellar structure and is prepared from aryl monomer having a pi-pi accumulation function and carboxyl monomer having a hydrogen bond function. The hydrogel of the invention controls a drug release system by a hydrogen bond and a pi-pi accumulation biswitch and realizes continuous regulation of drug release; the gel swelling property test shows that the hydrogel of the invention has favorable pH responsiveness; the drug release experiment stimulating a human body metabolic system shows that the drug release control system prepared by the hydrogel of the invention can match drug release and the human body metabolic system and effectively reduces drug waste and side effect on the human body by excessive drug.
CN1602872A Antituberculosis pharmaceutical composition The invention relates to an antituberculosis drug combination, prepared of rifampicin, isonicotinyl hydrazine, pyrazinamide, ethambutol hydrochloride and other auxiliaries, able to effectively overcome problems of drug resistance, improving compliance of patient, etc. It is applied in a compound form, which can avoid curing by single antituberculosis drug, thus avoiding selective drug resistance caused by single drug; the patients are willing to accept this, avoiding irregular drug application caused by simultaneously taking several drugs and different numbers of drug tablets, or taking more or less drugs.
CN101012211A Substituted andrographolide derivative, preparing method and pharmaceutical compound thereof The invention discloses a compound and medical acceptable salt with general formula (I) and making method and their drug agent, which possesses better COX-2 expressive inhibiting and TNF-alpha inhibiting and IL-6 inhibiting action.
WO2008022024A3 Imidazole amines as inhibitors of beta-secretase The present invention provides a compound of formula (I) and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ß-amyloid deposits or ß-amyloid levels in a patient (I).
US20110311632 Stable chitosan hemostatic external patch and methods of manufacture Hemostatic products with improved stability are prepared from crosslinked chitosan hemostatic compositions. The crosslinked chitosan hemostatic compositions have improved stability and can be prepared into a variety of medical devices in various shapes and sizes so as to be usable for inhibiting blood flow and ooze from substantially any type of bleeding site. For example, the chitosan compositions can be prepared into hemostatic gauze pads, bandages, wrappings, wound dressings, wound coverings, wound dressings, incision dressings, sealers, sheets, rolls, combinations thereof, and the like.
EP1194141B1 Antiviral therapy The invention relates to the field of antiviral agents, and more specifically to antiviral therapy. The invention provides use of at least one compound or mixture of compounds of general formula (I) or a functional equivalent or pharmaceutically acceptable salt or hydrate thereof for the production of a pharmaceutical composition for the treatment of a viral infection.
US20080146674 Composition for topical application comprising an antiseptic dye present in range of 0.005 to 0.05 weight percent, the dye being gentian violet, carbol fuschin dye, Castellani's paint and/or mixtures thereof; atopic dermatitis, skin irritation caused by S. aureus, rashes, psoriasis, eczema, stings, cuts A composition and method for treating a skin problem, particularly atopic dermatitis, the composition comprising an antiseptic dye, preferably gentian violet, in a vehicle effective for topical administration.
EP2311462A1 Method of preventing and treating airway remodeling and pulmonary inflammation using A2B adenosine receptor antagonists The present invention relates to methods of preventing airway remodeling using A2B adenosine receptor antagonists. This invention finds utility in the treatment and prevention of asthma, COPD, pulmonary fibrosis, emphysema, and other pulmonary diseases. The invention also relates to pharmaceutical compositions for use in the method.
US20060030900 Two-phase oxygenated solution and method of use A two-phase mixture is provided having a dissolved gas and a suspension of bubbles in a liquid. Methods for making, maintaining, and using the two-phase mixture are also provided. The gas molecules may be introduced into the liquid at a high velocity under elevated pressure to form a supersaturated solution that retains the dissolved gas concentration in solution when the solution is exposed to ambient conditions. The mixture may be used in a number of applications where high concentrations of gas must be retained in solution during prolonged exposure to ambient conditions. An example of use is the treatment of wounds to non-surgically remove dead, devitalized, contaminated and foreign matter from tissue cells. The mixture may be combined with a plastic to encapsulate the suspension of bubbles to minimize liberation of the gas bubbles from the mixture.
CN101230070A Novel anti-infection cephalosporin compounds The invention relates to a novel anti infectious cephalosporin compound shown in general formula (I), the pharmaceutically acceptable salt, the easily hydrolysable ester, the isomer, the hydrate and the hydrate of the salt or ester thereof, wherein, R1, R2, R3, R4, and X are defined as in the instruction; the preparation method of the compound, the medicine composition containing the compound and the use of the compound in preparing medicines for treating and/or preventing infectious diseases belong to the medicament technical field.
CN102349906A Atorvastatin calcium and nicotinic acid composition and preparation method thereof The invention discloses a 3-tier application pharmaceutical preparation of atorvastatin calcium and nicotinic acid composition and a preparation method thereof, such as tablets and capsule preparations, which is a slow-release layer composed of a nicotinic acid and an auxiliary material for release rate control, an isolation layer composed of excipients, and a quick-release layer composed of the atorvastatin calcium and pharmaceutical excipients. The nicotinic acid and the atorvastatin calcium are isolated by the isolation layer so as not to contact with each other, thereby avoiding interaction between the nicotinic acid and the atorvastatin calcium, achieving the long-term storage stability of the compound medicament preparation, and being favorable for the long-term storage of medicaments.
WO2006047931A1 The use of dipyridamole in manufacturing the anti-malignant tumor medicines The use of dipyridamole in manufacturing the anti-malignant tumor medicines, preferably solid type carcinoma, lung carcinoma, leukaemia and lymphoma. Dipyridamole can be formulated into capsule, tablet, powder, granule, oral liquid, injection and so on. When dipyridamole is formulated into capsule, tablet, powder and granule, the vehicle may be one of starch, dextrin, beta-CD and microcrystalline cellulose. The weight ratios of dipyridamole to starch, dextrin, beta-CD and microcrystalline cellulose are 1:5-15, 1:0.05-0.5, 1:0.01-0.5, 1:0.05-0.5 respectively. The inhibition ratio of dipyridamole to human leukaemia is 40-96%.
WO2006062732A3 Compounds acting at the centrosome The present invention relates to compounds, and methods utilizing compounds, which exhibit one or more of the following properties: i) disrupts organization of an actin cytoskeleton of a cell; ii) disrupts organization of a microtubule network of a cell; iii) induces accumulation of tubulin at centrosomes but does not induce accumulation of tubulin in a nucleus of a cell; iv) induces accumulation of tubulin at centrosomes at a concentration of 500 nM or less within four hours; v) induces accumulation of Hsp70 and has weak-to-moderate proteasome inhibitory activity; and vi) does not have proteasome inhibitory activity when assayed on purified proteasomes.
WO2010032974A2 Improved production method for adefovir dipivoxil The present invention relates to an improved production method for adefovir dipivoxil of Chemical formula 1. The production method according to the present invention is characterised in that dimethyl sulfoxide is used as a reaction solvent, and it comprises a process in which adefovir dipivoxil of Chemical formula 1 is produced by reacting adefovir of Chemical formula 2 with chloromethyl pivalate at between 30°C and 50°C in the presence of a solvent consisting of the dimethyl sulfoxide and triethylamine.
EP1322596B1 Zwitterionic tachykinin receptor antagonists The present invention is directed to certain novel compounds represented by structural formula (I), or a pharmaceutically acceptable salt thereof, wherein R?3, R5, R6, R7, R8, R11, R12, R13¿, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.
CA2062792C Treatment of androgen-related diseases A method of treatment of androgen-related diseases such as prostate cancer in susceptible male animals, including humans, comprises administering novel antiandrogens and novel sex steroid biosynthesis inhibitors as part of a combination therapy. Sex steroid biosynthesis inhibitors, especially those capable of inhibiting conversion of dehydroepiandrosterone (DHEA) or 4-androstenedione (.DELTA.4-dione) to natural sex steroids (and testosterone into dihydrotestosterone) in peripheral tissues, are used in combination with antiandrogens, usually after blockade of testicular hormonal secretions. Antiestrogens can also be part of the combination therapy. Pharmaceutical compositions and two, three, four and five component kits are useful for such combination treatment.
US20070265301 Dpp-IV Inhibitors The invention relates to compounds of formula (I), wherein Z, R1-8, n, A1, X1 and X2 have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.
CN1583004A Composition of cupresulflavone and its preparation A Ganxiang cypress' flavone composition used for preparing the medicine to treat tumor is prepared from the twigs and leaves of Ganxiang cypress through extracting in water, regulating pH-9-10, macroreticular resin adsorbing, eluting, extracting by butanol and concentrating.
CN103340849A Application of naringenin in preparing medicament for preventing and/or treating abdominal aortic aneurysm The invention discloses a novel medicament use of naringenin. The novel use disclosed by the invention is an application of naringenin in preparing products for preventing and/or treating abdominal aortic aneurysm. The products include a medicament and/or a health-care product. According to the application, two clinical-associated abdominal aortic aneurysm disease models are adopted, i.e., angiotensin II (1000ng/kg/min) subcutaneous implanted pump is used for inducing ApoE (apolipoprotein E) gene knockout mouse and calcium phosphate (0.5M) to paint C57 mouse abdominal aortic aneurysm locally induced by aorta abdominalis. The experiments prove that the naringenin is taken orally and lavaged can be used for remarkably inhibiting the generation and development of the mouse abdominal aortic aneurysm which is painted by CaPO4 and induced by the AngII (angiogenin II) implanted pump and can be used for treating a patient suffering from abdominal aortic aneurysm.
EP1272490B1 Sodium salt of an azo derivative of 5-aminosalicylic acid The present invention relates to the sodium salt of (Z)-2-hydroxy-5-[[4-3-[4-[2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)methyl]-1-piperidinyl]-3-oxo-1-phenyl-1-propenyl]phenyl]azo]benzoic acid, whose formula is shown below, as well as to the pharmaceutical compositions containing it, to a procedure for its preparation and to its use for the manufacture of medicaments for the treatment or prevention of inflammatory bowel disease.
WO2006052190A1 Indazole sulphonamide derivatives Compounds of formula I or pharmaceutically acceptable salts thereof: Formula (I) wherein R1, R2, R3 and R8 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
US20050181038 Novel method of stabilizing diagnostic and therapeutic compounds in a cationic carrier system The present invention relates to a method of stabilizing a low molecular weight compound in a cationic liposome, wherein said compound has a low solubility in a lipid membrane and/or a low permeability across a lipid membrane. Preferrably, the compound is modified in order to increase lipid membrane solubility and/or lipid membrane permeability. After delivery of the cationic liposome to a target site, particularly a target site in an organism, the modification is reversed and the low molecular weight compound may enact its desired activity.
US20120302630 Na/K-ATPase Ligands, Ouabain Antagonists, Assays and Uses Thereof Na/K-ATPase/Src ligands, assays and uses thereof are disclosed.
WO2010109736A1 Cartilage production promoter and prophylactic or therapeutic agent for diseases associated with cartilage damage Disclosed is a therapy which is for preventing or treating cartilage damage and diseases associated with cartilage damage, such as arthritides and osteoarthritis, and utilizes a more effective and more safe medicinal agent. Specifically disclosed are a cartilage production promoter, a glucosaminoglycan and/or proteoglycan production promoter, and a prophylactic or therapeutic agent for diseases associated with cartilage damage, each of which comprises fucoidan as an active ingredient.
US7476664 Bis-2-difluoro-pyrrolo[2,1-C][1,4]benzodiazepine dimers The present invention provides a novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula VII wherein, n is 3 to 10. novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula VII exhibits biding affinity with calf thymus (CT) DNA at a molar ratio of 1:5 in aqueous sodium phosphate buffer at pH of about 7.00. The present invention further provides a process for the preparation of novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula VII.
EP1966187A1 Piperazine compounds useful as antagonists of c-c chemokines (ccr2b and ccr5) for the treatment of inflammatory diseases A compound of formula (I) P - W - C(=X) - L - Q (I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y11 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.
CN103372014A Quickly dissolved-out stable vardenafil hydrochloride oral solid preparation and preparation method thereof The invention relates to a quickly dissolved-out stable vardenafil hydrochloride oral solid preparation and a preparation method thereof. The preparation uses a vardenafil hydrochloride trihydrate as an effective medicine, is served with auxiliary materials such as a filler, a disintegrating agent, an antioxygen, a corrigent, a flow aid and a lubricant, and adopts a pharmaceutically acceptable preparation process. According to the formula and preparation process provided by the invention, the dissolving-out speed of the oral preparation can be improved, the medicine is quickly released, and the stability of the medicine can be further improved.
CN102038698A New application of morroniside The invention discloses new application of morroniside, which provides the application of the morroniside in the preparation of medicines for treating or preventing sepsis. The intravenous injection of the morroniside can reduce the levels of sepsis rat serum HMGB1 (High-mobility Group-Box 1protein), TNF (Tumor Necrosis Factor)-alpha, IL (Interleukin)-6, endotoxin and TREM (Triggering Receptor Expressed on Myeloid Cells)-1.
CN1846695A Application of 3,5,7,3',4',5'-hexahydroxyl-2,3-dihydroflavone in preparing medicine The present invention relates to the new use of 3,5,7,3',4',5'-hexahydroxy-2,3-dihydroflavone in preparing medicine. The compound 3,5,7,3',4',5'-hexahydroxy-2,3-dihydroflavone is applied in preparing saccharification end product inhibitor, antioxidant and diacyl glycerol protein kinase C inhibitor.
US7666869 Nitrogen-containing 5-membered ring compound The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1: H, a lower alkyl group, etc., X: a single bonding arm, —CO—, -Alk-CO—, —COCH2—, -Alk-O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, -Alk-CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.
EP0888326B1 Novel ortho-naphthoquinone derivatives, novel synthesis therefor, and their use in the inhibition of neoplastic cell growth A novel synthetic method, novel compounds formed using the synthetic method, and uses for the compounds so made are described. The synthetic method results in the formation of o-naphthoquinone derivatives. These compounds find use as potent inhibitors of neoplastic cell growth and proliferation.
CN101390839A Policosanol drop pill and preparation method thereof The invention discloses policosanol dropping pills and the preparation method thereof, which prepare solid dispersoid through water-soluble substrate and enable the policosanol to be in the state of ultrafine particles, microcrystallines or molecular, so as to improve the dissolution quantity and dissolution rate. The state that the medicine dissolving property is good cannot always ensure the bioavailability is good; proper amount of surfactant-type absorption enhancer is added to the policosanol dropping pill preparation to improve the diffusion in the mucosal mucus layer in cellular membrane, so as to enable the policosanol dropping pill to quickly penetrate the biological membrane and increase absorption. The policosanol dropping pill and the preparation method have the advantages of high dissolution rate, high bioavailability, simple process, convenient product application and carrying, being applicable to the treatment of hypercholesterolemia, anti-platelet aggregation, ischemia, thrombosis and complications of atherosclerosis, improving the exercise performance and response sensitivity.
CA2125579C Ulcer prevention treatment composition and method Anti-ulcer compositions are disclosed having therapeutic agents dispersed in a soluble matrix formed by melt spinning the therapeutic agent with a carrier and hydrogel. Methods of treating ulcer-bearing tissue and preparing the matrix are also disclosed. One embodiment includes use of gastric irritating bio-affecting agents in which case the composition is preventative as well as therapeutic.
CN102988313A Anastrozole dispersible tablet and preparation method thereof The invention provides an anastrozole dispersible tablet and a preparation method thereof. The anastrozole dispersible tablet comprises a primary component which is anastrozole, and auxiliary components comprising a disintegrating agent, a filler, a flavoring agent and the like. The anastrozole dispersible tablet rapidly forms a uniform suspension after meeting water, has the characteristics of convenient administration, fast absorption, high biological availability and the like, can improve the compliances of patients, and can increase the clinical medication selection of doctors and the patients.
WO2010129524A3 Plant medicinal compounds The invention provides methods of extracting polyphenol compounds from botanical feed stocks. Also provided are food supplement compositions enriched in proanthocyanidins of type- A, including cinnamtannin Bl and related type- A trimers and tetramers, combined with extract of turmeric high in curcumin, as well as methods of using such compositions to treat diabetes mellitus and/or related diseases.
US20080058279 Such as 3-[4-(2-Octadec-9-enyloxycarbonyl-ethylamino)-butylamino]-propionic acid octadec-9-enyl ester dihydrochloride salt; use with vectors for in vivo transfection This invention relates to newly identified ester-linked Gemini surfactant compounds of formula (I), where Y is either H or (Aa)x where (Aa) is a basic amino acid and x is 1 to 6, to the use of such compounds and to their production. The invention also relates to the use of the ester-linked Gemini surfactant compounds to facilitate the transfer of polynucleotide into cells.
CN103340844A Application of gamatine in preparing drug resisting high PTH The invention discloses an application of gamatine in preparing a drug for preventing, alleviating and/or treating high PTH diseases. Gamatine is applied in preparing the drug for preventing, alleviating and/or treating the high PTH diseases. Experiments show that both experimental rabbits with parathyroids fully resected and experimental rabbits intragastrically administered with gamatine appear tonic spasm symptoms about 30 hours after the experiments; the PTH values in serum are obviously reduced; and the difference has a statistical significance, so that gamatine has a quite obvious inhibiting effect for secretion level of serum PTH of the rabbits; further, gamatine has an effect for rectifying high PTH; and particularly, the application of gamatine in preparing the drug resisting the high PTH allows the drug to be used for preventing, alleviating and/or treating the high PTH diseases.
WO2008148744A1 Thiadiazole derivatives as antidiabetic agents Novel compounds that are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of the present invention may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
WO2008060907A3 Pyrrolo-pyridine kinase inhibitors The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof. The Formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1 and IGFR-1, thereby making them useful as anti-cancer agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
CN101880281A Thiophane nucleoside analogues and preparation method and application thereof The invention discloses thiophane nucleoside analogues expressed as formulas A, A', B and B', or pharmaceutically acceptable salts, solvates, optical isomers or polymorphic substances thereof and a medicinal composition, wherein R represents H, halogen or methyl; R1 represents chain aliphatic alkyl of C1 to C3, cyclic aliphatic alkyl of C3 to C6, benzyl or substituted benzyl; and R2 represents hydroxy or amino. The invention also discloses a preparation method of the thiophane nucleoside analogues and application thereof in preparing a medicament for treating malignant tumor. The compounds of the invention have certain malignant tumor resistance and application values in the medicinal field.
CN102558255A Aminoglycoside compound and extracting and separating method thereof The invention relates to an aminoglycoside substance and an extracting and separating method thereof. The compound is separated from etimicin sulfate, and has a structural formula shown in the specification. The invention further relates to a separating method of the aminoglycoside substance.
EP2512240A1 Methods and compositions for treating and preventing trigeminal autonomic cephalgias, migraine, and vascular conditions The present invention relates to, among other things, methods for treating trigeminal cephalgias such as migraine and migraine like headaches and other cerebrovascular conditions associated with pain and or inflammation. When non-steroidal anti inflammatory drugs (NSAIDs), such as ketoprofen, are applied locally using specific topical formulations immediate relief of pain is obtained. Intense pain is typically reduced to mild pain or no pain within 30 minutes of application of the topical formulation. The NSAID may be given in combination with other pharmacological agents, such as vasoconstrictors, opioids, decongestants and/or non-opioid migraine drugs, such as triptans and ergots and agents that affect serotonin receptors as agonists, antagonists or partial agonists.
US20120157414 Cannabinoid receptor antagonists-inverse agonists useful for treating metabolic disorders, including obesity and diabetes The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.
US20080194548 combination of a CCR2 antagonist and a statin is useful in the treatment and or prevention of inflammatory and other disorders, and methods of treating inflammatory and other disorders using a combination of a CCR2 antagonist and a statin. A combination of a CCR2 antagonist and a statin is useful in the treatment and or prevention of inflammatory and other disorders, and methods of treating inflammatory and other disorders using a combination of a CCR2 antagonist and a statin.
CA2451932C Pyrrolopyrimidines as protein kinase inhibitors This invention is directed to compounds of the formula (I) to N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or solvates, to compositions comprising such compounds, and to methods of treatment comprising administering, to a patient in need thereof, such compounds and compositions.
CN103755585A Derivatives of ent-kaurenoid compounds, and preparation method and application thereof The invention relates to derivatives of ent-kaurenoid compounds, and a preparation method and application thereof. An ent dammara diterpenoid compound ent-dammara-16-ene-19-acid is extracted and separated from mangrove associate Wedelia prostrata, and structurally modified to synthesize the series derivatives of ent-kaurenoid compounds, which are disclosed as general formulae 1-4. The ent-kaurenoid compounds with alpha methylene ketone active functional group are obtained in the invention; and the experimental research indicates that the derivatives have favorable inhibitory activity for multiple human tumor cells, and therefore, can be used for preparing antineoplastic drugs.
WO2005110470A3 Methods and compositions for the modulation of immune responses and autoimmune diseases by activating rp105 (cd180) The present invention relates to a regulation of inflammation and immune responses. The present invention relates to a method of treating a condition comprising administering a pharmaceutically effective amount of an activator of RP105. The condition is typically associated with TLR-4 activation and cytokine production. Conditions addressed by the invention include sepsis, septic shock, inflammation, rheumatoid arthritis and Crohn's disease. The invention also provides the use of an activator of RP105 in the manufacture of a medicament for use in the treatment of a condition associated with cytokine production and methods for identifying an activator of RP105, which is also suitable for use in the treatment of a condition associated with stimulus-induced cytokine production. More specifically the patent relates to the use of RP105 as a specific inhibitor of TLR4 signaling and as a physiological regulator of TLR4 signaling for the treatment of TLR4-mediated inflammation and immune-related diseases. This invention also relates to treating a subject having a disease or condition associated with Toll-like receptor 4.
CN101601672A Application of penehyclidine hydrochloride oral cavity partial drug administration as dental surgery medicine The invention provides a new medical application of penehyclidine hydrochloride, mainly relating to the application of penehyclidine hydrochloride oral cavity partial drug administration as dental surgery medicine; the drug administration method adopted in the dental surgery is oral cavity partial drug administration, which can be either oral cavity spray method or oral cavity smear method. Penehyclidine hydrochloride can be prepared into pressurized sprays or can also be prepared into solutions.
CN101933920A Application of 3,15-dicarbonyl gibberellic acid methyl ester in reversing tumor multidrug resistance The invention relates to application of 3,15-dicarbonyl gibberellic acid methyl ester (GA) in reversing tumor multidrug resistance. A compound GA provided in the invention has favorable activity on the reversing tumor multidrug resistance (MDR), the GA acting on K562/A02 has higher drug susceptibility and can obviously reverse the drug resistance of the K562/A02 for ADM (Archer Daniels Midland); the effect mechanism of the GA for reversing the multidrug resistance of K562/A02 cells is realized by increasing the contents of chemotherapeutic drugs in the drug-resistance cells to prevent the chemotherapeutic drugs from being discharged outwards and promote the apoptosis of the drug-resistance cells, and has no obvious relevance with the expression of down-regulated drug-resistance genes mdr-1, thereby prompting that the action mechanism of the GA is relevant to the outward discharging pump function of inhibiting the drug-resistance cells P-gp and inducing the apoptosis of the drug-resistance cells; and the compound GA has lower toxicity, and therefore the compound GA has favorable application prospect on clinical tumor chemotherapy and particularly on resisting clinical tumor drug resistance.
EP1406899B1 Phenylacetamido-thiazole derivatives, process for their preparation and their use as antitumor agents Compounds represented by formula (I), as defined in the description, wherein R is a hydrogen atom or a methyl group and R1 is a group as defined in the specification, or a pharmaceutically acceptable salt thereof, are disclosed; the said compounds are useful in the treatment of cell proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
CA2251086C Glycopeptide compounds The present invention is directed to certain glycopeptide dimers in which two glycopeptide units are covalently linked to one another through their disaccharide amine, via a linking radical. This invention is also directed to the monomeric intermediates. All of these compounds are useful as antibacterials, especially for the control of gram positive bacteria; the compounds are particularly useful for the control of resistant bacterial strains, such as vancomycin-resistant-enterococci ("VRE").
CN101214245A Composition containing ciclacillin or its derivatives and preparation thereof The present invention provides a series of combination which contains ciclacillin or the derivative of the ciclacillin and is the combination essentially consisting of the ciclacillin or the derivative of the ciclacillin and an expectorant drug, wherein, the derivative of the ciclacillin is the officinal salt or officinal ester of the ciclacillin. The expectorant drug is any one of ambroxol, acetylcysteine, carbocisteine, erdosteine, fudosteine and lignum vitae glycerol ether. The unit medication dosage of the ciclacillin is 0.25g to 0.5g which is preferential (counted by active component), and the unit medication dosage of the expectorant drug is 0.01g to 2.0g. The combination is mainly used for remedying the respiratory tract infection with the symptom of expectoration.
CA2335623C Aminoiminoquinone and aminoquinine alkaloid compounds as capase inhibitors The subject application concerns novel compounds of structural formula (I) wherein R1 is NH or O; R2 is OZ; R3 is OZ; R4 is H or R; R5 is NH2, NR2, or OZ; and R6 is H or X; wherein Z is selected from the group consisting of H, R, COR, mesyl, tosyl, glutamyl, succinyl, and malonyl; R is selected from the group consisting of C1 to C8 alkyl, phenyl, and benzyl; and X is C1, Br, or I, with useful biological properties. For example, theses compounds can be used as anti-inflammatory, anti-proliferative, immunomodulatory, and/or neuroprotective agents. Specific examples of the compounds of the subject invention include Secobatzelline A and Secobatzelline B, which can be isolated from marine sponges.
CN101647936B Manufacture method of mouth care lozenges The invention belongs to nutrition and healthcare products, in particular to a manufacture method of mouth care lozenges. The manufacture method comprises the following steps: proportionally weighting, crushing and uniformly mixing aloe vera, mint, honeysuckle, forsythia, borneol and asarum; adding the mixture to a certain amount of water to be decocted; clarifying and filtering; condensing filtrate to obtain concentrate; weighing and adding a certain amount of gelatin, dextrin and sugar syrup to the concentrate, uniformly stirring so as to prepare wet particles; and drying and tabletting thewet particles to prepare products. The product can effectively clear halitosis, relieve and stop pain, effectively clear oral bacteria, prevent various oral diseases and has special effects on the treatment of toothache.
US20110064715 Methods for determining oligosaccharide binding The invention relates to methods for detecting and characterizing enzymatic modifications of oligosaccharides, such as heparan sulfate, and their interaction with binding partners, such as proteins, using an oligosaccharide-binding partner binding assay, such as a gel mobility shift assay. The instant invention relates to a rapid, convenient, sensitive and inexpensive method for identifying or studying oligosaccharide-binding partner interactions, identifying and characterizing structural features on oligosaccharides, identifying and characterizing binding partners, identifying agents capable of interfering with, enhancing, or facilitating the binding of an oligosaccharide to its binding partner, diagnosing conditions associated with altered oligosaccharide-binding partner binding, and generating oligosaccharide libraries and kits therefor.
CN100589812C Plant worms mycelium extracat fraction and composition for oral intake The invention provides a fraction containing the active ingredient contained in plant worms. The invention also provides a means efficacious in immunopotentiation, an effective means of preventing ortreating cancer and a composition useful in producing health foods. It is intended to provide a precipitation fraction obtained by extracting plant worms mycelium with hot water and adding ethanol tothe thus obtained extract. It is also intended to provide a composition for oral intake which contains the above precipitation fraction. It is further intended to provide foods, drinks, immunopotentiators, anticancer agents and so on containing the above composition for oral intake which are characterized by having an anticancer effect, an effect of preventing cancer or an immunopotentiation effect. It is furthermore intended to provide a method of effectively producing the above-described composition for oral intake.
EP1962842A1 Diaryl ureas for treating inflammatory skin, eye and/or ear diseases The present invention relates to pharmaceutical compositions for treating inflammatory skin, eye and/or ear diseases comprising at least a diaryl urea compound optionally combined with at least one additional therapeutic agent. Useful combinations include e.g. BAY 43-9006 as a diaryl urea compound.
US20100266700 Use of adsorbent carbon microspheres for the treatment of irritable bowel syndrome Adsorbent carbon microspheres are administered to treat irritable bowel syndrome or symptoms associated with irritable bowel syndrome.
CN101336936A Compound thrombolytic and pericardium clearing complex capsule and preparation method thereof The invention provides a compound capsule with thrombolytic and heart meridians dredging effects and a preparation method thereof. The compound capsule is prepared from hirudo and aspirin. The hirudo is Hirudo nipponia artificially fed in a special pond, which has a flat and long cylindrical shape, is composed of multiple segments, has five yellow-brown colored lines, and has a dark green-colored or black-brown colored back; or Whitmania pigra which has a flat spindle shaped and is composed of multiple segments. The preparation method comprises the steps of: collecting hirudo, suffocating, washing with clear water, air-drying or oven-drying, crushing, sieving to obtain powder, and sterilizing; and collecting aspirin which is odorless pure white crystalline powder with sourish taste, mixing the hirudo powder and aspirin at a weight ratio of 18:1, mixing, stirring, encapsulating with a specification of 475 mg, and packaging. The inventive compound capsule can be used for preventing cerebrovascular sclerosis, cardiovascular sclerosis, increase of blood viscosity, cerebral thrombosis, severe breast pain caused by angina pectoris and myocardial infarction, etc.
CN1981865A Formula and usage for treating acne A medicine for treating scar is composed of three components which are mixed before it is applied. It is proportionally prepared from hyaluronidase, lactose, azoanthracene, purified water, triamcinolone, refined lavenda oil, and ethyoxylated hydrogenated lanolin.
US7220742 For therapy of respiratory complaints The present invention relates to enantiomerically pure compounds of general formula 1 wherein the groups R1, R2, R3, R4 and X− may have the meanings given in the claims and in the specification, processes for preparing them and the use thereof as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.
CN103622968A Application of tozasertib in preparation of drug for treating glaucoma disease The invention discloses a novel application of tozasertib and analogous compounds of tozasertib or pharmaceutical salts of tozasertib, and the novel application is an application in preparation of drugs for treating glaucoma disease. The tozasertib and analogous compounds of tozasertib or pharmaceutical salts of tozasertib can be made into normal preparations and long-acting preparations. The preparations mentioned above have a very prominent effect on glaucoma treatments.
WO2011073437A2 Bacteriocin- and prebiotic-based cosmetic or dermatological compositions The invention relates to compositions containing, in a physiologically acceptable medium, the combination of at least one bacteriocin and at least one prebiotic. The invention also relates to the cosmetic uses and methods that implement the combination of a bacteriocin with a prebiotic.
CN101371846B Liquid medicine for curing burn and preparation method thereof The invention relates to a liquid medicine for treating burn; the liquid medicine is prepared by the following ingredients in terms of part by weight: 90-110 portions of prednisone tablets, 70-110 portions of maleate chlor-trimeton tablets, 180-220 portions of vitamin B1 tablets, 13-17 portions of dexamethasone tablets, 5-8 portions of chloramphenicol eyedrop and 90-110 portions of distilled water. In preparation, all ingredients are taken in proportion; prednisone tablets, maleate chlor-trimeton tables, vitamin B1 tablets and dexamethasone tablets are dissolved in distilled water or smashed before being dissolved in distilled water, added with chloramphenicol eyedrop and evenly mixed. The antibiotic, anti-flammatory and anti-allergic functions of the liquid medicine can ensure the burnt skin does not be invaded by external bacteria and keep the cleanness, so that the burnt skin can be healed in a short time; the liquid medicine can be used for treating burn, scald, cauterized wound, and on the like, has the advantages of low treatment cost, short healing time, and no scar, and can also be used for treating tympanitis with good curative effect.
CA2844907A1 Concentrated felbamate formulations for parenteral administration Formulations of a neuroprotective agent for parenteral administration are described herein. The formulation is in the form of a concentrated (supersaturated) solution or a concentrated suspension of microparticles. The suspension medium or the solution solvent carrier may also contain dissolved neuroprotective agent. For the supersaturated solutions, the agent is dissolved at high concentrations of at least about 1% by weight, 5% by weight, 10% by weight, 15% by weight, or 20% by weight in a solvent suitable for parenteral administration. For the concentrated suspension, the microparticles have an effective particle size from about 100 nm to about 5 microns, preferably from about 50 nm to about 3 microns, more preferably from about 10 nm to about 2 microns. The formulations described herein can be used to treat a variety of neurological diseases/disorders and/or neurological injury or trauma.
US20100292309 Inducing immune-mediated tumor cell death This document provides methods and materials related to treating cancer. For example, methods and materials that include using CD40L polypeptide, an hsp70 polypeptide, and a cytotoxic polypeptide to trigger an immune response directed against cancer cells are provided.
US7332493 [3-Methyl-4-(pyridin-3-yloxy)-phenyl]-(6-piperidin-3-ylethynyl-quinazolin-4-yl)-amine; selective inhibitors of receptor tyrosine kinases and non-receptor tyrosine kinases (eg: Ick, src, abl) or serine/threonine kinases (e.g.: cyclin dependent kinases); carcinoma The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R5, R11, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
US7332517 1-(1H-indol-3-ylmethyl)-3-(4-nitrophenyl)-5-[2-(4-phenyl-1H-imidazol-2-yl)ethyl]-2thioxo-4imidazolidinone; somastatin receptor affinity; acromegaly, hypophyseal adenomas, endocrine gastroenteropancreatic tumors, as carcinoid syndrome and gastrointestinal bleeding A method of treating a disorder selected from the group consisting of acromegaly, hypophyseal adenomas, endocrine gastroenteropancreatic tumors including carcinoid syndrome and gastrointestinal bleeding in warm-blooded animals comprising administering to warm-blooded animals in need thereof an amount of a compound of the formula in racemic or enantiomeric form.
US20120129761 Preparation of bone cement compositions A method for the preparation of injectable ready-to-use paste bone cement compositions by mixing a dry inorganic bone cement powder comprising a particulate calcium sulfate hemihydrate capable of hardening in vivo by hydration of the calcium sulfate hemihydrate forming calcium sulfate dihydrate, an aqueous liquid and an additive that normally retards the setting process, said method comprising a) providing a bone cement powder comprising calcium sulfate hemihydrate, an accelerator for the hardening of the calcium sulfate hemihydrate by hydration, said accelerator being selected from the group consisting of saline and calcium sulfate dihydrate, and a powdered calcium phosphate component b) mixing the bone cement powder with the aqueous liquid for a period of time c) leaving the mixture for the time needed for allowing the hydration reaction of the calcium sulfate hemihydrate to proceed and allowing calcium sulfate dihydrate crystals to form and grow, and d) admixing the additive by means of a short-duration mixing using a minimum of energy surprisingly shortens the setting times for the cement comprising the additive that retard the setting process to the level observed in the absence of the additive and enables a complete hydration of calcium sulfate hemihydrate to calcium sulfate dihydrate, even when using additives else preventing the hardening.
US20100047326 Multiple-Compartment Applicator A multiple-compartment ascorbic acid delivery unit is provided. The first compartment is impermeable to oxygen and ultraviolet light and contains a solid vitamin-containing composition comprising ascorbic acid or its pharmaceutically acceptable salts and esters. The second compartment is liquid impermeable and contains a pharmaceutically acceptable carrier system. The first compartment is entirely enclosed within said second compartment or vice versa. An opening is formed in the inner compartment in order to combine the contents of the two compartments to form an ascorbic acid carrier composition prior to delivery to the patient.
US7049438 Quinazoline derivatives for treatment of tumours The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease
CN102863338A Compound and medical use thereof The invention discloses a new-found compound and medical use thereof. The compound is characterized in that structural modification is performed on salvia miltiorrhiza salvianolic acid A. The new compound with good stability and membrane permeability and high bioavailability is screened out through stability tests, limit of proportionality (Lop) determination, pharmacodynamic experiments and the like. The compound has better pharmacologic action in treatment of cardiovascular and cerebrovascular diseases and the like.
EP2255802A1 Adhesive skin patch and packaged product A patch 1 comprising a backing layer 2 and a pressure-sensitive adhesive layer 3 formed on the backing layer 2, wherein the pressure-sensitive adhesive layer 3 contains (i) ropinirole and a metal salt produced by the reaction of a ropinirole acid adduct and a metal ion containing desalting agent in an equivalent mole or less to the acid adduct and (ii) an adhesive base free of a hydroxyl group and a carboxy group.
CN102204885A Preparation method of aceglutamide glucose injection The invention belongs to the field of medical preparations, and in particular relates to a preparation method of an aceglutamide glucose injection. The preparation method of the aceglutamide glucose injection comprises the following steps of: (1) preparing a thick glucose solution, regulating the pH thereof to be 4.5-5.5; (2) preparing a thick aceglutamide solution, regulating the pH thereof to be 4.5-5.5; and (3) combining the two thick solutions prepared in steps (1) and (2), adding active carbon for decoloring, and supplementing water for injection to full dose. Because the pH of the thick glucose solution and the pH of the thick aceglutamide solution are regulated to the required values and then the two thick solutions are combined, the reaction speed of the glucose and the aceglutamide is reduced, and the reaction time of the glucose and the aceglutamide under a stronger acidic condition is reduced. The aceglutamide glucose injection prepared by the method provided by the invention has few related substances and good stability.
USRE41151 Comprising a modified NSAID, wherein the NSAID is covalently attached either directly or through a linker molecule to a sulfur-containing functional group containing an optionally substituted hydrocarbyl moiety; nonsteroidal anti-inflammatory drugs; side-effect reduction In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.
US20130012473 Combined use of phospholipid and sulfate groups-carrying polysaccharides for inhibiting metastatic spread The invention relates to a medicament comprising a phospholipid component and a polysaccharide component having polysaccharides containing sulfate groups for inhibiting metastatic spread of tumors. The two components may be in same or separate preparation.
CN102988367A Application of tetrandrine in hepatic stellate cell migration inhibition drug preparation The present invention discloses an application of tetrandrine in hepatic stellate cell migration inhibition drug preparation. According to the present invention, a PDGF-induced human hepatic stellate cell line (LX-2) migration screening platform is designed, and results show that PDGF-induced hepatic stellate cell (HSC) migration can be inhibited with 10<-4>-10<-7> mol/L tetrandrine.
US20080194659 Cinnamic, Phenylpropiolic and Phenylpropanoic Acid Derivatives Useful as Anti-Tumor Agents Cinnamic and phenylpropiolic acid derivatives of formula (I) having antitumour and chemo sensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.
WO2012004917A1 Neurite outgrowth agent Disclosed is a non-peptide-type nerve axon/neurite outgrowth agent which can extend a nerve axon or a neurite. 3-(Aminocarbonyl)-1-[5-O-[[1-(6-amino-9H-purin-9-yl)-1- deoxy-β-D-ribofuranos-5-O-yl]phosphonyloxy(oxylato)- phosphinyl]-β-L-ribofuranosyl]pyridinium, which is a nicotinamide adenine dinucleotide (NAD) analogue containing a β-L-ribose as a constituent sugar, can be used as a nerve axon and/or neurite outgrowth agent or composition, a proliferation inhibitor or an apoptosis inducer for a cancer cell, or a proliferation inhibiting composition or an apoptosis inducing composition for a cancer cell.
EP2545924A1 Method for the prevention and treatment of sepsis. This invention is in the field of medical treatment, in particular the invention provides a method for the prevention and treatment for sepsis or septic shock. The invention provides a novel use of a known medicament, i.e. pentasaccharide-depleted heparin for use in the treatment or prevention of sepsis, SIRS, severe sepsis or septic shock.
US20120064099 Compounds that inhibit nfkb and bace1 activity The present invention relates to compounds with activity as BACE1 and NFκB modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds.
WO2008072360A1 Catechin composition and method for producing the same It is intended to provide a catechin composition with less unpleasant bitterness although containing unpolymerized catechins at a high concentration. When the weight ratio of the content of (A) gallate type catechins to the content of (B) unpolymerized catechins [(A)/(B)] is in the range of from 0.50 to 0.75, the weight ratio of the content of (B) the unpolymerized catechins to the content of (C) total polyphenols [(B)/(C)] is in the range of from 0.80 to 0.97, the weight ratio of the content of (D) a flavonol aglycone to the content of (B) the unpolymerized catechins [(D)/(C)] is less than 0.002, the weight ratio of the content of (E) caffeine to the content of (B) the unpolymerized catechins [(E)/(C)] is less than 0.1 and the CPA value of an aqueous solution measured by a CPA method using a C00 type sensor is 5 µV/ppm or higher in terms of the concentration of the unpolymerized catechins, it can be provided as a catechin composition with less unpleasant bitterness although containing unpolymerized catechins at a high concentration.
CN101455715B Suppository for treating gynecologic diseases and preparation method thereof The invention relates to a suppository for treating gynecopathy and preparation method thereof. The suppository is obtained by the steps of processing raw materials and auxiliary materials such as sophora root, pearl layer powder, dried alum, quassia wood, cnidium seed, berbamine hydrochloride, menthol, borneol, boracic acid, seabuckthorm seed oil, and mixed fatty glyceride. Compared with presenttechnology, the inventions has better curative effect, nonirritant, and no toxicity and side effect mainly and the invention is applied to treatment for vaginitis, cervicitis and cervical erosion having good effectiveness and high curative rate.
US20120022067 Thiazole and oxazole-substituted arylamides as p2x3 and p2x2/3 antagonists Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
CN102153515A N,N'-bis-substituted urea Raf kinase inhibitors and preparation method and application thereof The invention relates to the field of pharmaceutical chemistry, in particular to N,N'-bis-substituted urea compounds, a preparation method thereof, a medicinal composition containing the compounds and medical application of the N,N'-bis-substituted urea compounds, particularly application of the N,N'-bis-substituted urea compounds used as a Raf kinase inhibitor.
CN102764248A Application of teprenone in prevention and treatment of morphine-induced liver injury The invention relates to a new application of teprenone in preparation of a medicament for preventing and treating morphine-induced liver injury, and discloses teprenone capable of protecting liver cells from being poisoned by morphine, inhibiting morphine-induced cell apoptosis and weakening morphine-induced lipid per-oxidative injury. The teprenone can be used for preventing and treating the morphine-induced liver injury.
CN103169706A Compound oral disintegrating tablet containing acetaminophen and dextromethorphan The invention relates to the field of pharmaceutical preparation, and in particular relates to a compound oral disintegrating tablet containing acetaminophen and dextromethorphan hydrobromide. The compound oral disintegrating tablet contains the following components of: a. acetaminophen and dextromethorphan hydrobromide coating particles, wherein the particle diameter of the coating particles is 60-100 meshes, the coating particles contain particles including acetaminophen and dextromethorphan hydrobromide, a coating material coated on the particle surface, and the coating material comprises ethylcellulose and at least one pore-foaming agent; b. a filler which is directly compressible mannitol, mannitol, microcrystalline cellulose or a mixture thereof; c. a disintegrating agent selected from crospolyvinylpyrrolidone or croscarmellose sodium; d. a lubricant which is talcum powder or magnesium stearate; and e. an effervescing agent.
CN102908388A Formosan lattuce herb buccal tablet A formosan lattuce herb buccal tablet belongs to the field of health care products. The formosan lattuce herb buccal tablet comprises 3%-10% of broadleaf holly leaf, 0.02%-0.5% of potassium sorbate, 15%-40% of dextrin, 1%-5% of peppermint powder, 15%-28% of mannitol powder, 0.45%-4.95% of newtol, 3%-10% of momordica grosvenori and 0.01%-0.1% of borneol. The formosan lattuce herb buccal tablet has the advantages of being low in manufacture cost, slow in dissolving after entering a mouth and capable of moistening the laryngeal and the esophagus for a long time, and having effects of clearing heat, refreshing and clearing and nourishing throat.
WO2009076321A2 Compositions and methods for modulating gene expression using asymmetrically-active precursor polynucleotides The present invention is directed to novel nucleic acid molecules which include a region complementary to a target gene and one or more self-complementary regions, and the use of such nucleic acid molecules and compositions comprising the same to modulate gene expression and treat a variety of diseases and infections.
US20080176849 e.g. N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]-amino]methyl]phenyl]-2E-2-propenamide; histone deacetylase inhibitor; anticarcinogenic, antitumor, antiproliferative agents; improved stability The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.
WO2009158487A2 Treatment of nephrolithiasis and urolithiasis using 1,2,3,4,6-penta-o-galloyl-beta-d-glucose (pgg) The treatment of nephrolithiasis or urolithiasis by methods that include administration of 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG) or a salt or derivative thereof, or a pharmaceutically acceptable composition comprising the same are provided herein.
EP1143970B1 Pyridine compounds, use and preparation thereof New pyridine compounds are provided along with their method of preparation. The compounds are useful as intermediates in preparing new anticancer agents. A few of the pyridine compounds are also useful for treating cancer.
CN102440998A Compound doxycycline hyclate suspension injection and preparation method thereof The invention discloses a compound doxycycline hyclate suspension injection and a preparation process thereof. The suspension injection is prepared by taking doxycycline hyclate and tilmicosin phosphate as main medicines and adding appropriate medical accessories. The compound doxycycline hyclate suspension injection comprises the following components: 5-20 percent (W/V) of doxycycline hyclate, 5-20 percent (W/V) of tilmicosin phosphate, 0.5-2 percent (W/V) of a suspending aid, 0.01-0.2 percent (W/V) of an antioxidant, 0.1-2 percent (V/V) percent of a thickening agent and injection oil which supplements the balance to reach 100 percent. According to the invention, the doxycycline hyclate and the tilmicosin phosphate are evenly suspended into a solvent by a special process, and therefore the compound doxycycline hyclate suspension injection has good dispersibility and high bioavailability. Meanwhile, a feasible approach is provided for broadened production, and the advantages of increasing medical efficacy, reducing medication frequency and saving manpower and material resources are achieved.
WO2010138101A1 Combination therapy for the treatment of multiple myeloma using cep-18770 together with bortezomib or mephalan The present invention provides a method for treating multiple myeloma in a subject, comprising the step of administering to the subject a combination of COMPOUND 1 and bortezomib. The invention further provides a method for treating multiple myeloma in a subject, comprising the step of administering to the subject a combination of COMPOUND 1 and melphalan.
CN101888877A Pyridine derivatives for the treatment of amyloid-related diseases a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein X and Y are independently NR5 or O; W and Z are independently a bond or (CH2)mCH(R7)(CH2)n; m = 0-1, n = 0-2; R is hydrogen or halogen; R1and R2 are independently selected from hydrogen, halogen, CF3, CN, OR8, NR9R10, NR9COR11, NR9SO2R11 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R3 is hydrogen, halogen, CF3, CN, OR8, SR8 or SO2R 11.; R4 is hydrogen, halogen, CF3, OR9, NR9R10, NR9COR11, NR9SO2R11 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R5 is hydrogen or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10;R6 is hydrogen, fluorine, C1-6 alkyl, or C1-6 alkoxy; R6 is hydrogen, fluorine, C1-6 alkyl, or C1-6 alkoxy; R7 is hydrogen, C1-6 alkyl, phenyl or C1-3 alkylphenyl wherein said phenyl groups are optionally substituted by one or more substituents selected from halogen, C1-6 alkyl, CF3, OCF3 or OR9; R8 is hydrogen or C1-6 alkyl optionally substituted by fluorine, C1-6 alkoxy or NR9R10; R9 is hydrogen, C1-6 alkyl or C1-3 alkylphenyl wherein said phenyl group is optionally substituted by one or more substituents selected from halogen, C1-6 alkyl, CF3, OR8, NR9R10Or OCF3; R10 is hydrogen, C1-6 alkyl, C1-6 alkenyl, phenyl or C1-3 alkylphenyl wherein said phenyl groups are optionally substituted by one or more substituents selected from halogen, C1-6 alkyl, CF3, OR8 or OCF3; or the groups R9 and R10 when they are attached to a nitrogen atom may together form a 5- or 6-membered ring which optionally contains one further heteroatom selected from NR9, S and O; and R11 is C1-6 alkyl or a phenyl group optionally substituted by one or more substituents selected from halogen, C1-6 alkyl, CF3, OCF3 or OR8 is provided. The compounds are useful in treating amyloid related diseases.
WO2011002184A2 Phosphoric acid ester of bicalutamide for treating prostate cancer Provided is a phosphoric acid ester of bicalutamide and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient for treating prostate cancer, with which a linear correlation between the systemic exposure to bicalutamide and the dosage level can be achievable, making it possible to increase the bioavailability of bicalutamide upon oral administration at a high dosage level.
US20120101140 Econazole Composition and Methods of Treatment Therewith The invention provides a water-based composition for treating an infection by a dermatophyte fungus comprising econazole or a pharmaceutically acceptable salt thereof. Also provided are methods of treatment utilizing the water-based foam composition, as well as its preparation.
US20100120776 Carbocysteine medical foods Medical foods containing carbocysteine and designed for buccal absorption; useful for treating conditions that benefit from administration of an antioxidant, immunostimulant, and/or mucoregulator, such as COPD.
US20080045500 Nerve Regeneration Stimulator A nerve regeneration stimulator comprising a compound having a cholinesterase inhibitory activity, a pharmacologically acceptable salt thereof or a solvate thereof.
US20080200479 Acid moiety selected from pyroglutamic acid, N-(2-carboxyphenyl)-glycine acid, diglycolic acid, orotic acid, galactaric acid, nicotinic acid, hippuric acid; treatment of nervous system disorders such as schizophrenia, obsessive compulsive disorder, bipolar depression, anxiety, mania, Tourette syndrome The invention relates to new salts of ocaperidone and uses thereof, particularly in the pharmaceutical industry. The invention discloses specific salts of ocaperidone having increased water solubilities, as well as therapeutic methods by administering said salts, in particular for treating various diseases of the central or peripheral nervous system, especially central nervous system. It further deals with pharmaceutical compositions comprising said salts and methods for preparing the same.
WO2009050252A1 Novel sulfamate compounds for medical use This invention relates to sulfamates of Formula (I), wherein R1 to R3 and n are defined in the claims, having carbonic anhydrase enzyme inhibitory activity, to medicaments comprising these compounds, to pharmaceutical compositions comprising these compounds, and to processes for the preparation of these compounds. The invention is also directed to the use of such compounds, medicaments and compositions, particularly to their use in administering them to patients to achieve a therapeutic effect.
CN103055322A Targeted sustained release medicine carrying nanoparticle and preparation method thereof The invention discloses a targeted sustained release medicine carrying nanoparticle and a preparation method thereof. A mixture of a carrier I containing tumor targeted molecules and a carrier II containing antineoplastic drugs serves as a carrier of the nanoparticle, an organo-siloxane reagent easily hydrolyzed serves as a silane coupling reagent, and the nanoparticle which has a core-shell structure including that drugs are wrapped in the core through chemical bond connection and in a physical mode and the targeted molecules are exposed outside is obtained through micro emulsion technical preparation. The drugs are wrapped on the nanoparticle through a chemical method and the physical method, the mass fraction of the drugs in a nanoparticle is increased, preliminary-stage release is slowed down, and later-stage release is supplemented. The organo-siloxane reagent forms another layer of shell on a macromolecule two-block interface layer due to strong hydrolysis of the organo-siloxane reagent and the characteristic that the organo-siloxane reagent and a hydrophilic chain of amphipathy block polymers easily form hydrogen bonds, and therefore the effect of slow-release is strengthened.
CN101961484A Prostate secretory protein 94/57 (Psp94/57), analogous polypeptides thereof for preparing medicaments for eliminating drug (therapy) resistance of tumor, and application thereof The chemical drug and radiation therapy is an effective conventional method for treating cancers, but in the process of cancer treatment, the produced drug (therapy) resistance causes the effectiveness thereof to be reduced quickly and even disappear, so the drug (therapy) resistance is the biggest obstacle to the successful cancer treatment. The invention provides a medicament composition and a preparation method thereof, which can cause part of drug (therapy) resistance of tumor to disappear, thereby restoring the sensitivity of cancer cells to the original treatment method, namely, the medicaments combined with chemotherapy or radiotherapy can effectively treat the cancers which have produced drug (therapy) resistance. The medicament composition and method use human secretory proteins 94/57 or short peptides synthesized based on the amino acid sequence of the secretory proteins 94/57, and analogous polypeptides subjected to processing and modification to eliminate the drug (therapy) resistance of tumor and treating cancers through combining with commonly-used chemotherapeutics or radiotherapy.
CA2357744C Potassium salt of (s)-omeprazole The present invention relates to a novel form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H--benzimidazole, known under the generic name omeprazole. More specifically, it relates to a novel crystalline form of the potassium salt of the (S)- enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole. The present invention also relates to processes for preparing such a form of the potassium salt of (S)- omeprazole and pharmaceutical compositions containing it.
CN102895194A Methods for the preparation of biologically active compounds in nanoparticulate form A method for producing a composition comprising nanoparticles of a biologically active compound.
US7642261 Treating bipolar disorder, mania, dementia, sexual dysfunction, eating disorders, fibromyalgia 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof is used for the manufacture of a medicament for the treatment of sub-type anxiety disorders chosen from the sub-types panic disorder with or without agoraphobia, agoraphobia obsessive-compulsive spectrum disorders, social phobia, posttraumatic stress disorder, acute stress indication or generalized-anxiety disorder, bipolar disorders, mania, dementia substance-related disorders, sexual dysfunctions, eating disorders, obesity, anorexia and fibromyalgia. A preferred salt is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride.
US20090062347 Deuterated axitinib (AG-13736), N-Methyl-2-[[3- [2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl]sulfanyl]benzamide; cancer treatment The present application describes deuterium-enriched axitinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN102366405A Fluticasone propionate aerosol preparation with hydrofluoroalkane as propellant The invention discloses a fluticasone propionate aerosol preparation with hydrofluoroalkane as a propellant. The preparation comprises a curatively or prophylactically effective amount of fluticasone propionate, or a pharmaceutically acceptable salt or solvate thereof, and a hydrofluoroalkane propellant. Fluticasone propionate or the pharmaceutically acceptable salt or solvate thereof is a granular medicine processed through spray drying. The aerosol preparation provided by the invention is a medical aerosol preparation with good stability. The aerosol preparation can be produced through a one-step or two-step canning method.
CN103242392A Novel glycyrrhizic acid double salt, and preparation and application thereof The invention belongs to the field of chemical raw materials, and discloses a novel glycyrrhizic acid double salt, and preparation and application thereof. The invention relates to a preparation method of a glycyrrhizic acid double salt, which comprises the following steps: dissolving glycyrrhizic acid or soluble glycyrrhetate thereof in water or a water-ethanol mixed solution, meanwhile, respectively dissolving a soluble silver salt and a soluble zinc salt in water or a water-ethanol mixed solution, and dissolving by stirring at 10-95 DEG C in a dark place; and mixing the three salt solutions to react, thereby obtaining the zinc silver glycyrrhetate white precipitate. In the invention, the glycyrrhizic acid or soluble salt thereof is combined with necessary microelement zinc for the human body and silver ions with broad-spectrum sterilizing effect for the first time; different activity action mechanisms of the glycyrrhizic acid or soluble salt thereof, zinc and silver ions are utilized to perform the functions of diminishing inflammation, killing bacteria, resisting viruses and restoring normal functions of histiocytes; and the glycyrrhizic acid double salt can be used for preparing medicines for diminishing inflammation and killing bacteria on the skin surface, or medicines for promoting restoration of mucous membranes and epithelial tissues as well as wound healing, and can also be used for preparing a washing-type personal nursing system.
WO2014016233A1 Compositions comprising hyaluronic acid and dermatan sulphate for the treatment of being overweight and obesity The present invention relates to a composition comprising hyaluronic acid and dermatan sulphate for use in the treatment or prevention of overweight, obesity, insulin resistance, type 2 diabetes, fatty liver or dyslipidemia or for use in reducing food intake, inducing the feeling of satiety, reducing appetite, reducing body weight, preventing weight gain, reducing body fat, reducing fat formation, reducing blood cholesterol, maintaining normal blood cholesterol levels, reducing blood triglycerides, maintaining normal blood triglyceride levels or increasing insulin sensitivity. The composition can further contain collagen hydrolysate. The composition can be in the form of a pharmaceutical composition, a food, a functional food, a medical food or a food supplement.
WO2013064029A1 Benzoylurea derivative with anticancer activity and preparation method and use thereof Provided in the present invention are a benzoylurea derivative of formula (I) with anticancer activity or the pharmaceutically acceptable salt or prodrug thereof, and the preparation of such a derivative and the use thereof in preparing a drug for treating diseases relating to a poly(ADP-ribose)polymerase(PARP) inhibitor, such as a drug for treating a cancer.
US20090252757 Methods and compositions for inhibiting hiv infection This invention provides novel HIV-interacting host factors. The invention also provides methods of using the HIV-interacting host factors to screen for compounds that inhibit HIV infection. The methods comprise first screening test compounds for modulators of an HIV interacting host factor disclosed herein, and then further screening the identified modulating compounds for ability to inhibit HIV infection. The invention further provides methods and pharmaceutical compositions for treating diseases and conditions associated with HIV infection.
CN101851209B Imidazole ethyl vanillic acid ether, preparation method and medicinal application thereof The invention relates to the field of medicine, in particular to the compound of imidazole ethyl vanillic acid ether (I), a preparation method, pharmaceutical composition containing the compound and medical application thereof. The compound I of the invention has prevention and treatment effects on cardiovascular diseases caused by platelet aggregation, particularly has strong inhibitory effect on platelet aggregation induced by ADP on the basis that the compound I does not prolong bleeding time.
US20110144041 Methods for Treating Inflammatory Bowel Disease A method is described for treating inflammatory bowel disease in a subject in need thereof. The method comprises administering a formulation comprising at least one ganglioside to the subject, wherein the formulation comprises at least about 50% GD3 by weight of total ganglioside content.
CN103070879A Application of hyperin in preparing anti-ovarian-senescence drug The invention discloses an application of hyperin in preparing an anti-ovarian-senescence drug. The hyperin can treat multiple ovarian senescence diseases, such as a polycystic ovarian syndrome, dysfunctional uterine bleeding, premature ovarian failure and a climacteric syndrome, and has a significant effect. According to the application, the hyperin is administrated orally, percutaneously or by injection for treating the ovarian senescence diseases.
US6986905 Pharmaceutical compositions for treating and saving and the method for the preparation thereof The present invention relates to a pharmaceutical composition and the method for the preparation thereof, The composition comprises 1.5˜6.9% (w/v) of one or more substances selected from sodium chloride, sodium bicarbonate, potassium chloride, magnesium sulfate, calcium chloride, calcium gluconate, and the like, and 3˜18% (w/v) of one or more substances selected from hydroxyethylstarch, dextran, carboxymethylstarch, polyvinyl-pyrrolidone, gelatin derivatives, and the like as well as the remainder of conventional injections, as long as sodium chloride is not less than 1.5% (w/v). The pharmaceutical composition of the present invention is used to treat and save the wounded and patients, as well as to treat shock, its advantages include safe and convenient use, rapid and good curative effect, long time maintenance, extensive uses and the like.
WO2014121901A1 Polymorphic forms The present invention relates to novel salt forms with improved manufacturability and solid-state properties of [6-Fluoro-1-(4-morpholin-4-ylmethyl-phenyl)-5,5-dioxo-4,5- dihydro-1 H-5l6-thiochromeno[4,3-c]pyrazol-3-yl]-morpholin-4-yl-methanone, and to methods of their manufacture.
WO2005047282A1 Antiresorptive mutual salt of raloxifene and bisphosphonic acid The mutual salt of raloxifene and bisphosphonic acid exhibits unexpectedly synergistic effects of two components to enhance bone mineral density (BMD), control blood-calcium density, and lower the serum cholesterol level.
EP2703387A1 Cyclohexyl-substituted piperazine compounds The present invention relates to cyclohexyl-substituted piperazine, piperidine and cyclohexane compounds, composition comprising the same and process for their synthesis. The invention also relates to said compounds for use as medicament, in particular for the treatment and/or prevention of early stage of Alzheimer's disease.
US20090221547 Immunosuppressant Compounds and Compositions The present invention relates to immunosuppressants, processes for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction. This application relates to compounds selected from Formula (Ia), (Ib), (Ic) and (Id).
CN101486772B Mistletoe polysaccharide, as well as preparation and use thereof A mistletoe polysaccharide consists of glucose, arabinose, galactose, glucuronic acid and galacturonic acid, with the molecular weight of 1.1 multiplied by 10<6>-3.4 multiplied by 10<6>Da, the terminal group carbon of Alpha-configuration, and the specific rotation of [Alpha]D being equal to plus 134.6 degrees to plus 167.3 degrees; and the basic skeleton of the polysaccharide consists of 1-5 glycosidic bond connected Arab sugar and 1-6 glycosidic bond connected galactose. The mistletoe polysaccharide is obtained by water extraction and alcohol precipitation, an ion exchange chromatography and a molecular sieve chromatography by further purification. The mistletoe polysaccharide has obvious inhibition action on Hela cells and mouse transplanted tumors S-180, so the polysaccharide can beused for preparing drugs for treating cancer.
US20060241133 Electrically variable pneumatic structural element There is disclosed the use of a compound of formula (I): or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the treatment of age-related cognitive decline or mild cognitive impairment, in particular with a view to preventing or delaying the onset of Alzheimer's disease.
US20070244080 Method for Treatment of Inflammatory Disorders Using Triptolide Compounds Inflammatory disorders, including obliterative airway disease, renal fibrosis, diabetic nephropathy, and liver fibrosis are treated with immunosuppressive triptolide compounds, in particular triptolide compounds effective to inhibit TGF-β production in a patient afflicted with such a disorder.
WO2007014940A8 Quinoline derivatives as antibacterical agents Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib), a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2 or 3; R2 is hydrogen; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of Formula (ΙΙ); R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is zero, 1, 2, 3 or 4; X is a direct bond or CH2; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen or a radical of Formula (III); R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo ; or R8 and R9 together form the radical -CH=CH-N=.
US20130239239 Lmcd1 cancer markers and methods for their use The present invention provides LMCD1 cancer markers, and methods, compositions, and kits for their use. The invention also provides expression vectors, host cells, and transgenic animals comprising one or more LMCD1 mutations, and methods for their use in characterizing, diagnosing, and treating cancers, and for identifying potential therapeutics. The invention also provides cancer therapeutics.
WO2008008513A2 Combination treatments The present invention relates to the treatment of disorders using pharmaceutical agents in combination with heme oxygenase- 1 and/or heme degradation products, such as biliverdin or carbon monoxide.
WO2008041914A1 5-(2-AMINO-L-HYDROXYETHYL)-8-HYDROXY-2-OXOQUINOLINE DERIVATIVES AND OTHER COMPOUNDS AS β2 -ADRENERGIC AGONISTS The present invention provides 5-(2-amino-l-hydroxyethyl)-8-hydroxy-2-oxoquinoline derivatives and other compounds of formula (I) wherein R1 is formula (A) wherein R4, R5 and M1 are as defined in the specification, or R1 is as defined in the specification, and wherein R2, R3, W, A, X and Y are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or conditions in which modulation of β2 adrenoreceptor activity is beneficial, e.g. adult respiratory distress syndrome (ARDS), pulmonary emphysema, bronchitis, bronchiectasis, chronic obstructive pulmonary disease (COPD), asthma or rhinitis. The compounds are β2-adrenergic agonists.
US20120207784 Insertion of foreign genes in rubella virus and their stable expression in a live, attenuated viral vaccine Disclosed herein are isolated rubella viral vector constructs that include a rubella non-structural protein open reading frame (ORF) with an in-frame deletion, a rubella structural protein ORF, and a heterologous antigenic insert. In one example, the in-frame deletion within the rubella non-structural protein ORF is an in-frame deletion between two NotI restriction enzyme sites. In some examples, the heterologous antigenic insert is positioned within the rubella non-structural protein ORF. In other examples, the heterologous antigenic insert is positioned within the rubella structural protein ORF. Exemplary antigenic inserts include a Gag antigenic insert, a gp41 antigenic insert or a gp120 antigenic insert. Also disclosed are uses of the isolated rubella viral vector, such as to induce an immune response to HIV-1, testing sensitivity to neutralizing antibodies, or screening antiviral drugs (such as protease inhibitors).
WO2012014848A1 Flavoniod-derived hes-1 promoter inhibitor [Problem] To provide an HES-1 promoter inhibitor which has strong HES-1 promoter inhibitory activity and which is less toxic to neural stem cells. [Solution] An HES-1 promoter inhibitor which comprises a compound represented by the general formula or a derivative thereof.
CN102525999A Ketotifen fumarate sustained-release capsules and preparation method thereof The invention discloses ketotifen fumarate sustained-release capsules and a preparation method thereof. The ketotifen fumarate sustained- release capsules comprise sustained-release pellets and hollow capsules, and each sustained-release pellet comprises 75-77% (by weight) of ketotifen fumarate-containing pellet core and 3-35% (by weight) of sustained-release layer. The ketotifen fumarate sustained-release capsules of the invention have uniform pellet diameter and stable drug release, can be released in a sustained manner within 24 hours, and are administered once every day. As the sustained-release pellets in the capsules comprise a plurality of pellets of uniform size, the errors or defects in preparation of individual pellets do not have a strong impact on drug release of the entire preparation, the ketotifen fumarate sustained-release capsules are safer than sustained-release tablets, and have smaller irritation to gastrointestinal tract, more stable blood concentration and higher bioavailability. The preparation method of the invention adopts an extrusion rolling method and a drug coating method to prepare the drug-containing pellet cores, and adopts a fluidized bed to coat the sustained-release coat layers; and has simple process, and is easy for industrial production.
EP2725013A1 Novel histone deacetylase inhibitor of benzamides and use thereof Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
CN101669953A Methionine vitamin B1 pharmaceutical composition for injection The invention relates to a methionine vitamin B1 pharmaceutical composition for injection, which is characterized in that the composition and the proportion of components are as follows: methionine: 100mg, vitamin B1: 10mg, glutathione: 5mg, BHA: 2mg, propylene glycol: 25mg, and water for injection: 5ml.
CN101112359A Method for preparing transparent water-dispersible concentrated liquor of beta-carotin The present invention discloses a preparation method of transparent water-dispersible-typed beta-carotene concentration liquid, which pertains to the technical field of food processing. The technic proposal includes: beta-carotene extract is dissolved in the edible oil to get the oil phase; the water and the propylene glycol are mixed in the proportion of 5:1 to 9:1 to get the water phase; the oil phase is mixed with Tween 80 or Tween 60 or Tween 40 emulsifier in the proportion of 6:1 to 2:1 firstly, and is then mixed with the water phase after being mixed for 20 to 40 minutes by an oscillator; the water phase accounts for 50 percent to 70 percent of the total volume, and the oil phase through the simple emulsification accounts for 50 percent to 30 percent of the total volume. The emulsification time is 0.5 to 2 hours, and the emulsification temperature is 28 to 40 DEG C. The usage of the method can change the beta-carotene from oil-soluble into water-soluble, so as to have good solubility and water dispersible property, stable nature and difficult oxidation, which can meet the different production needs.
CN103724198A Novel derivative of dimethyl fumarate and application of novel derivative The invention discloses a novel derivative of dimethyl fumarate and application of the novel derivative. The novel derivative has good medicine activity, can greatly prolong the half-life period of a medicine, prolongs the retention time of the medicine in a human body, and meanwhile, improves the concentration of the medicine in blood; therefore, better curative effect is achieved. As the half-life period of the medicine is greatly prolonged, activity concentration of the medicine in the blood can be maintained for a longer period of time; under the cure condition of dose constrain, the curative effect is maintained and the dosage of the medicine is reduced, so that the problem of bad metabolism of the medicine is eliminated, the medicine toxicity is reduced, and the toxic and side effects in the medicine use process are reduced.
US20110293740 Treatment system and method for osteopenia and osteoporosis using non-synthetic bio-available compounds A treatment system and method for osteopenia and osteoporosis using non-synthetic bio-available hormones, vitamins, minerals, and agents may be customized by varying the dosage and formulation of the components to maximize therapeutic effect, bioavailability, and patient comfort and compliance with their treatment method, the treatment system including a storage unit including a determined number of applications of hormones, minerals, and vitamins of appropriate dosages for treating the patient with osteopenia and osteoporosis.
US6844189 Chromosome 17P-linked prostate cancer susceptibility gene The present invention relates generally to the field of human genetics. Specifically, the present invention relates to methods and materials used to isolate and detect a human prostate cancer predisposing gene (HPC2), some alleles of which cause susceptibility to cancer, in particular prostate cancer. More specifically, the present invention relates to germline mutations in the HPC2 gene and their use in the diagnosis of predisposition to prostate cancer. The invention also relates to presymptomatic therapy of individuals who carry deleterious alleles of the HPC2 gene. The invention further relates to somatic mutations in the HPC2 gene in human prostate cancer and their use in the diagnosis and prognosis of human prostate cancer. Additionally, the invention relates to somatic mutations in the HPC2 gene in other human cancers and their use in the diagnosis and prognosis of human cancers. The invention also relates to the therapy of human cancers which have a mutation in the HPC2 gene, (including gene therapy, protein replacement therapy, protein mimetics, and inhibitors). The invention further relates to the screening of drugs for cancer therapy. Finally, the invention relates to the screening of the HPC2 gene for mutations, which are useful for diagnosing the predisposition to prostate cancer.
US20100272660 Cosmetic or pharmaceutical composition comprising a polycondensate, the said polycondensate and method of cosmetic treatment The present application relates to a cosmetic or pharmaceutical composition comprising a polycondensate capable of being obtained by the reaction of the following monomers alone: of 10 to 30% by weight, relative to the total weight of the polycondensate, of one or more polyols comprising 3 to 6 hydroxyl groups; of 30 to 80% by weight, relative to the total weight of the polycondensate, of one or more linear, branched and/or cyclic, saturated or unsaturated, non-aromatic monocarboxylic acids comprising 6 to 32 carbon atoms; of 1 to 40% by weight, relative to the total weight of the polycondensate, of one or more polycarboxylic acids and/or cyclic anhydrides of such a polycarboxylic acid and/or lactones comprising at least one COOH group; and optionally of 0.1 to 15% by weight, relative to the total weight of the polycondensate, of one or more silicones having a hydroxyl and/or carboxyl functional group. The application also relates to a method of cosmetic treatment using the said composition, and the polycondensate thus defined.
EP2401268A1 Oxyindole derivatives with motilin receptor agonistic activity The present invention relates to novel oxyindole derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the motilin receptor (GPR38).
EP1897864A1 Anthracene derivatives and the use thereof for treating benign and malignant tumors Anthracene derivatives (I), are new, where (I) excludes e.g. 10-((E)-1-benzoyl-3-phenyl-allylidene)-10H-anthracen-9-one with chemical abstract service (CAS) registry no. of 262378-52-9, 10-(1-benzoyl-3-phenyl-prop-2-ynylidene)-10H-anthracen-9-one with CAS registry no. of 121747-08-8 and 10-[1,2-bis-(4-methoxy-phenyl)-2-oxo- ethylidene]-10H-anthracen-9-one with CAS registry no. of 63370-49-0. Anthracene derivatives of formula (I), are new, where (I) excludes 10-((E)-1-benzoyl-3-phenyl-allylidene)-10H-anthracen-9-one with chemical abstract service (CAS) registry no. of 262378-52-9, 10-(1-benzoyl-3-phenyl-prop-2-ynylidene)-10H-anthracen-9-one with CAS registry no. of 121747-08-8, 10-[1,2-bis-(4-methoxy-phenyl)-2-oxo-eth ylidene]-10H-anthracen-9-one with CAS registry no. of 63370-49-0, 10-(2-oxo-1,2-diphenyl-ethylidene)-10H-anthracen-9-one with CAS registry no. of 19661-62-2, 10-(2-Oxo-2-phenyl-ethylidene)-10H-anthra cen-9-one with CAS registry no. of 17665-75-7, 2-(4,5-dihydroxy-10-oxo-10H-anthracen-9-ylidene)-succinic acid dimethyl ester with CAS registry no. of 83498-19-5, 10-(2-oxo-1-phenyl-propylidene)-10H-anthracen-9-one with CAS registry no. of 42866-43-3, 10-(1-methyl-2-oxo-propylidene)-10H-anthracen-9-one with CAS registry no. of 3095926 and 10-(2-oxo-1-phenyl-butylidene)-1 0H-anthracen-9-one with CAS registry no. of 42866-49-9. X : O, S, NR 1> 1>, N-OR 1> 2>, geminal bonded hydrogen or OH; Y 1>O, S, NR 1> 3> or N-OR 1> 4>; R 1>-R 8>H, optionally substituted (cyclo)alkyl, optionally substituted cyclodialkyl, optionally substituted heterocycle, optionally substituted heterocycle-alkyl, optionally substituted aryl, optionally substituted aryl-alkyl, optionally substituted heteroaryl, optionally substituted heteroaryl-alkyl, amino, mono-alkylamino, di-alkylamino, F, Cl, Br, I, alkyl with one or more substituted F atoms, trifluoromethyl, CN, cyano-alkyl, carbonyl, carboxyl, COOH, alkoxycarbonyl, carboxy-alkyl, alkoxycarbonyl-alkyl, OH, alkoxy, aryl-alkoxy, benzyloxy, heteroaryl-alkoxy, alkoxycarbonylamino or alkoxycarbonylamino-alkyl; R 9>optionally substituted (cyclo)alkyl, optionally substituted cyclodialkyl, optionally substituted heterocycle, optionally substituted heterocycle-alkyl, optionally substituted (hetero)aryl, optionally substituted aryl-alkyl, optionally substituted heteroaryl-alkyl, -OR 1> 5> or -1NR 1> 6>R 1> 7>; R 1> 0>H, optionally substituted alkyl, optionally substituted (hetero)aryl, optionally substituted aryl-alkyl or optionally substituted heteroaryl-alkyl; and R 1> 1>-R 1> 7>H, optionally substituted (cyclo)alkyl, optionally substituted cyclodialkyl, optionally substituted heterocycle, optionally substituted heterocycle-alkyl, optionally substituted (hetero)aryl, optionally substituted aryl-alkyl or optionally substituted heteroaryl-alkyl. Independent claims are included for: (1) the preparation of (I); (2) a pharmaceutical composition comprising (I); and (3) a medicament comprising (I). [Image] - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : Tubulin polymerization inhibitor; Microtubuli-based motor protein inhibitor. The tubilin polymerization inhibitory activity of (I) was tested in-vitro. The results showed that the EC 5 0 value of 10-[2-(3,4-dihydroxy-phenyl)-2-oxo-ethylidene]-10H-anthracen-9-one was 7.15/8.02 mu g/ml.
CN102743754A Esophagus gastrointestinal mucosa protective adhesive preparation and its application The invention relates to a protective adhesive preparation, concretely speaking relates to an esophagus gastrointestinal mucosa protective adhesive preparation containing an immunomodulator. The esophagus gastrointestinal mucosa protective adhesive preparation is composed of the immunomodulator, hyperoxia methyl pectin, a pH value conditioning agent and an adhesive agent. The immunomodulator preferably selects an acellular short corynebacteria preparation. The invention also relates to the application of the esophagus gastrointestinal mucosa protective adhesive preparation for protecting esophagus gastrointestinal mucosa, which comprises the applications of medicines and/or health products preparation for treating esophagitis, gastritis, gastric ulcer, enteritis and intestinal tract ulcer. and applications of the medicines and/or preparations preparation for minimizing burning sensation on stomach due to alcohol or gastric acid, burning sensation due to gastric acid esophagus countercurrent flow, restoration for lower end of the damaged esophagus.
WO2012101292A1 1,2,4-oxadiazole derivatives as drugs modulating the glp-1 peptide receptor The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, when preparing a drug for preventing and/or treating a disease which involves the GLP-1 receptor, such as eating disorders and illnesses; for instance: obesity, anorexia, lipid dysfunction, diabetes, hyperinsulinism and cardiovascular diseases or metabolic syndrome.
CN101961324A Prescription and preparation method of etofbrate release capsules The invention provides a prescription and a preparation method of etofbrate release capsules. The prescription comprises a main medicament and an enteric material. Pattern drawing is performed by adopting enteric ethanol or ethanol-acetone solution of methacrylic acid copolymer, polyacrylic resin or phthalic acid ethyl cellulose so as to capsule the etofbrate into small pills with release characteristic; and then the small coated pills are filled in enteric empty capsules.
US20080233222 Method of Improving Cardiovascular Health A nutritional supplement including β-cryptoxanthin is found to be effective at lowering blood pressure in mammals. β-cryptoxanthin therefore may be used to maintain cardiovascular health by lowering blood pressure, preventing high, elevated blood pressure and/or maintaining healthy blood pressure. Administration of β-cryptoxanthin in combination with safflower oil is particularly effective.
WO2009017236A1 Pyridopyrimidin-4-one derivatives Pyridopyrimidin-4-one derivatives represented by the general formula (1) or pharmaceutically acceptable salts thereof have arginine vasopressin 1b receptor antagonism and are useful as therapeutic or preventive agents for depression, anxiety, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune related diseases, depilation, and so on.
US7256201 Selective estrogen receptor-β ligands The invention relates to novel compounds having the general formula: (I) and arc useful as selective ER-β ligands in the treatment or prophylaxis of Alzheimer's disease, anxiety disorders, depressive disorders, osteoporosis cardiovascular disease, rheumatoid arthritis or prostate cancer.
WO2009067543A2 Treatment of histone deacetylase mediated disorders Provided herein are pharmaceutical agents, pharmaceutical compositions, methods of treatment, treatment regimens and kits for the treatment of histone deacetylase mediated disorders.
US20080114055 By using [3-(3,4-Dimethyl-9-oxo-9H-thioxanthen-2-yloxy)-2-hydroxypropyl]trimethyl-ammonium chloride to reduce or reverse cachexia or disease-induced body weight loss One embodiment of the invention uses thioxanthone compounds containing a choline or choline analogue moiety, such as CCcompound1 or [3-(3,4-Dimethyl-9-oxo-9H-thioxanthen-2-yloxy)-2-hydroxypropyl]trimethyl-ammonium chloride, to reduce or reverse body weight loss in various mouse models of human tumors. Another embodiment of the invention discloses a method for reducing or reversing cachexia or disease-induced body weight loss in human and other mammals using thioxanthone compounds containing a choline analogue moiety.
US20090220562 Osteogenic and anti-adipogenic oxysterols The present invention discloses osteogenic and anti-adipogenic oxysterols. Agents and methods for protecting, blocking or rescuing marrow stromal cells from the inhibitory effects of oxidative stress on their osteoblastic cellular differentiation are disclosed. Exemplary agents include oxysterols alone or in synergistic combinations, as well as hedgehog or Wnt signaling activators. The synergistic effects of oxysterols and bone morphogenic proteins are also disclosed.
US20100169989 Use of Follistatin-Like Related Gene (FLRG) to Increase Muscle Mass The present relates to use of follistatin-like related gene (FLRG) to increase muscle mass in a subject. As such, methods of ameliorating the severity of a pathologic condition characterized, at least in part, by a decreased amount, development or metabolic activity of muscle are provided. In addition transgenic non-human mammals expressing FLRG and having increased muscle mass as compared to a corresponding mammal having a myostatin-null mutation or a decreased level of myostatin are provided.
US20110287026 Sirt4 and uses thereof Provided herein are SIRT4 compositions and methods of use thereof. The invention provides functional information for use in the identification and design of compounds that modulate SIRT4 enzyme activity (e.g., inhibition of fatty acid oxidation, ADP ribosylation, and/or downregulation of glutamate dehydrogenase), and to the compounds identified by such methods and the research, diagnostic and therapeutic uses of such compounds.
CN1965854A Moisturizing eye drop and preparation process therof The invention relates to a method for preparing eyedrops, wherein the invention is characterized in that: adding 98.0-99.2% injection water into container, 5-10%.common salt, 0.1-0.2%. acid sodium phosphate, 1-3%. acid sodium phosphate, to prepare buffer liquid; when they are dissolved completely, adding 0.01-0.10% hyaluronic acid, 0.10-1.00% chitosan, mixing; using 0.22 mum filter element to disinfect and filter in multistage room, using machine to automatically pack. The invention can accelerate the growth of epithelial cell, and it will not flow into nasal. It not contains conservative and antibacterial agent.
CN101863898B Thieno pyridinone derivative containing piperazidine and preparation method and applications thereof The invention belongs to the technical field of antineoplastic medicines and provides thieno pyridinone derivative with the structure of the general formula I and salt thereof which are acceptable in pharmacy, wherein n, R1 and R2 are defined in the specification. The invention also relates to a preparation method of the compound, and discloses pharmaceutical composites using the compound or the salt thereof which are acceptable in pharmacy as active ingredient and the applications of the pharmaceutical composites used as the antineoplastic medicines.
US20050014941 Cyanoalkylamino derivatives as protease inhibitors The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.
US20090048242 (1,10b-dihydro-2-(aminoalkyl-phenyl)-5h-pyrazolo[1,5 c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as hiv viral replication inhibitors The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.
CA2530345A1 Composition and method for mitigating a negative effect of alcohol consumption A composition for the prevention and treatment of symptoms (for example, a hangover) associated with ethyl alcohol consumption. The composition may comprise a gingerol, a silymarin, a catechin, and a group B vitamin. Treatment of symptoms associated with the consumption of ethyl alcohol may comprise administration of the composition prior to, during, or after the consumption of the alcohol.
US6958335 Use of imatinib, 4-(4-methylpiperazin-1-ylmethyl)-N-(4-methyl-3-(4-pyridin-3-y l) pyrimidin-2-ylamino)phenyl)-benzamide or a pharmaceutically acceptable salt 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of the formula I or a pharmaceutically acceptable salt thereof can be used in the treatment of gastrointestinal stromal tumours.
US7410984 novel pyridone derivatives capable of inhibiting alpha 4 integrin mediated cell adhesion; to treat chronic inflammatory diseases; 3-(4-{2-Oxo-3-[4-(3-o-tolyl-ureido)phenyl]-2H-pyridin-1-ylmethyl}phenyl)propionic acid; hydrolysis The present invention relates to novel pyridone derivatives capable of inhibiting α4 integrin mediated cell adhesion, processes for their preparation, compositions comprising them and their use in the treatment of diseases capable of being modulated by the inhibition of cell adhesion.
WO2012097222A1 High drug load tablet formulation of brivanib alaninate The present invention is directed to a high drug load tablet formulation of [ (1R), 2S] - 2 - aminopropionic acid 2 - [4 - (4 - fluoro- 2 -methyl - 1H- indol - 5 -yloxy) - 5 -methylpyrrolo [2, 1 - f] [1,2,4] triazin- 6 -yloxy] - 1 -methylethyl ester, and to methods of using the formulation in the treatment of cancer. The tablet is obtained by means of a wet granulation process.
CN103230376A Simvastatin tablet preparation method The invention relates to a simvastatin tablet preparation method, and belongs to the field of statin medicine tablet preparation methods. The tablets are composed of simvastatin and auxiliary materials such as a filling material, an adhesive, a disintegrant, an antioxidant, a lubricant, and the like. The method is characterized in that compressible starch is adopted as the adhesive and the disintegrant, and the mass ratio of simvastatin to the compressible starch is 1: (0.5-1.5). The invention mainly solves a problem of simvastatin tablet dissolution stability, such that simvastatin dissolution curve is S-shaped. During dissolution, an in-vitro slow intermediate-release characteristic is shown. The release characteristic satisfies clinical requirements, and assists in providing a good hypolipidemic effect. The preparation method provided by the invention has the advantages of simple process, feasible operation, and suitability for large-scale productions.
CN103191052A L-alpha-glycerol phosphorylcholine injection composition and preparation method thereof The embodiment of the invention discloses an L-alpha-glycerol phosphorylcholine injection composition. The L-alpha-glycerol phosphorylcholine injection composition comprises the active pharmaceutical ingredient, namely 1.0kg of L-alpha-glycerol phosphorylcholine per 1000 injections and 4L of water for injection per 1000 injections. The invention further discloses a preparation method of the L-alpha-glycerol phosphorylcholine injection composition, which comprises the following steps of: weighing the active pharmaceutical ingredient, namely the L-alpha-glycerol phosphorylcholine according to the formula amount, adding part of the water for injection according to the formula amount, stirring and dissolving; adding activated carbon for injection, adsorbing and filtering to remove the carbon; adding the remaining water for injection into a solution, and performing fine filtration by using a sterile microporous filter membrane; inspecting a semi-finished product, and filling and sealing after the semi-finished product is inspected to be qualified; performing hot pressing and sterilization; and inspecting a finished product and packaging. The formula and the preparation method have the advantages of reasonable parameters, maturity, stability, good reproducibility and stable product quality, and are suitable for large-scale production.
CN101224193A Compound sustained release injection containing newborn blood vessel inhibitor and cytotoxic drugs The invention relates to a compound sustained-released injection containing a neovascularization inhibitor, which comprises sustained-release microspheres and menstruum; wherein, the sustained-release microspheres are composed of sustained-release excipients, the neovascularization inhibitor selected from marimastat or fumagillin, etc. and a cytotoxic drug selected from hydroxyl campto thecine, mitozolomide, 4-carboxyl temozolomide, docetaxel, oxaliplatin, hetaplatin, ifosfamide, lomustine, estramustine, fotemustine, samustine, etoposide, teniposide, vinblastine, anastrozole, fluorouracil or mitomycin C. The menstruum is special menstruum containing a suspending agent. The sustained-release excipients are selected from polifeprosan, polylactic acid, decanedioic acid polymer, such as poly (erucic acid dipolyme-decanedioic acid) and poly (allomaleic acid-decanedioic acid), etc. and EVAc, etc; the suspending agent, the viscosity of which is 100cp-3000cp (between 25 DEG C and 30 DEG C), is selected from carboxymethylcellulose sodium, etc. The sustained-release microspheres can also be prepared to be a sustained-release implant. The sustained-release implant is injected or deposited to the interior of tumour or around the tumour, which can improve the treatment effect of non-operative treatments, such as radio-chemotherapy, etc.
US20100311719 Prevention of Obesity in Antipsychotic, Antidepressant and Antiepileptic Medication O-(3-piperidino-2-hydroxypropyl)-nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof (BGP-15) can be used for the prevention or reduction of weight gain or obesity in a patient treated with an antipsychotic drug or an antidepressant drug or an antiepileptic drug.
WO2008108647A2 Enhancement of anticancer therapy by flavonoids The present invention provides means and methods for the treatment of an individual suffering from cancer. A group of polyp henolic flavonoids where found to have synergistic anti-tumor activity with a chemotherapeutic drug.
EP1597258B1 Novel purine derivatives, preparation method thereof, application of same as medicaments, pharmaceutical compositions and novel use The invention relates to novel products having formula (I), wherein: Y represents N, O, S, CHR3 or =CR3; the dotted lines represent a single or double bond; R and R1 represent, in particular, H, Hal, OH, alkyl, alkoxy, cyano, NO2, NR4R5, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, -S(O)n-NR4R5, whereby n represents 0 to 2, acyl, -NH-CO-alkyl or -NH-CO-NH-phenyl; R3 represents H, Hal, alkyl, cyano, NO2, NR4R5, trifluoromethyl or aryl; R2 represents R4, OR4, SR4 or NR4R5; and R4 represents H, alkyl, cycloalkyl or aryl. According to the invention, either R4 and R5 are selected from among the values of R4, or R4 and R5, together with N, form a heterocyclic radical which can contain N, 0 and S, all of said radicals being optionally substituted. Moreover, the aforementioned products take all of the isomeric and salt forms for use as medicaments.
CN103751106A Water-soluble perfluorooctyl bromide-liposome nanosphere and preparation method thereof The invention relates to a water-soluble perfluorooctyl bromide-liposome nanosphere with a mean grain size of 30-800nm, the water-soluble perfluorooctyl bromide-liposome nanosphere structure is formed as follows: inner layer perfluorooctyl bromide (PFOB) is coated with outer layer lecithin bilayer to form a liposome nanosphere, the perfluorooctyl bromide-liposome nanosphere is negative in surface charge and is good in water-soluble property, an outer coating layer of the water-soluble perfluorooctyl bromide-liposome nanosphere is the well-biocompatible lecithin bilayer which can degrade in vivo, may not produce toxic and side effects on human body, the perfluorooctyl bromide-liposome nanosphere can be used as ultrasound diagnostic reagents and blood substitutes, and the particle size is easy to control and regulate, so that the application field is expanded. The preparation process of the perfluorooctyl bromide-liposome nanosphere is very simple in operation and low in requirement on equipment, and can be used for continuous production.
WO2013177633A1 Combination therapy involving a vascular disrupting agent and an agent which targets hypoxia The present invention provides a method for treating a proliferative disease in a patient. The method comprises administering to a patient in need thereof: a) a vascular disrupting agent and (b) at least one hypoxia targeting agent. Preferred combinations are BNC105 and Pazopanib and BNC 105 and Bortezomib.
EP1094822B1 Water miscible azalide solutions Water miscible pharmaceutical compositions containing up to about 40 % of a macrolide such as an azalide antibiotic are prepared by reaction of the macrolide with acid in a non-aqueous water miscible organic solvent system.
WO2011144054A1 Dibenzocyclooctene lignan derivatives and uses thereof in treatment of viral hepatitis Provided are dibenzocyclooctene lignan derivatives having the following structural formula and their uses in the treatment of viral hepatitis. Said dibenzocyclooctene lignan derivatives have bioactivity of anti-hepatitis B virus (anti-HBV) and are expected to be used in the preparation of anti-HBV drugs.
CN1813676A Anthracene ring antitumor medicinal liposome and its production process The present invention discloses an anthracyclic anti-tumor medicine liposome and its production process. It is composed of anthracyclic medicine, liposome material and antioxidant, the medicine/liposome ratio (w/w) is 0.05-0.2:1, in which the liposome material includes phospholipids and cholesterol, the mole ratio of both them is 40-60:30-50 mol%; the antioxidant is formed from alpha-tocopherol and desferal, their concentractions respectively are 0.010-0.030 mg/ml and 0.05-0.30 mg/ml. Its production process includes the following steps: (1). Preparing multiplayer liposome; (2), preparing small single-layer liposome; and (3), preparing anthracyclic medicine liposome.
CN101507714A Oral preparation containing 7,9-dihydroxy-15-carbonyl-16-kaurene -19,6-lactone The invention discloses an oral preparation containing 7,9-dihydroxyl-15-carbonyl-16-kaurene-19,6-lactone. The oral preparation is characterized in that: the oral preparation comprises the 7,9-dihydroxyl-15-carbonyl-16-kaurene-19,6-lactone used as an active component and auxiliary materials in portion by weight: 1 to 100 portions of 7,9-dihydroxyl-15-carbonyl-16-kaurene-19,6-lactone and 1 to 500 portions of auxiliary material; and the oral preparation can be one of a tablet, a capsule, a drop pill, a pelletized granule, a gelatin pill, a dry suspension, an otic gel or powder. The oral preparation containing the 7,9-dihydroxyl-15-carbonyl-16-kaurene-19,6-lactone has the advantages of stable and controllable quality, convenient taking, safety and effectiveness, economy and practicality, good product appearance and obvious curative effect of resisting tumors.
CN101732602B Medicament for treating calculi and preparation method thereof The invention discloses a medicament for treating calculi and a preparation method thereof. The medicament comprises the raw materials in percentage by weight: chicken gizzard-membrane, stir-fired antlion, spora lygodii, cluster mallow fruit, longhairy antenoron herb, lalang grass rhizome, beautiful sweetgum fruit, grassleaf sweelflag rhizome, prepared twotooth achyranthes root, cicada slough, talcpowder, astragalus, szechwon tangshen root and liquoric root. The raw materials of the medicament have abundant source and are readily available. Compared with the conventional formula and means fortreating urolithiasis and intra-hepatic cholelithiasis, a medicinal formula of the medicament is close to pathological change; and clinical tests prove that the medicament has the advantages of little dosage, short course of treatment, obviously curative effect and convenient administration, no need of surgical pain and no toxic or side effect, plays a role of preventing calculi regeneration, andpromotes to achieve the effects of eliminating dampness and heat and dissolving and removing calculi through conditioning of Chinese patient medicaments. In addition, the medicament is simple and convenient to produce and wide in application, and is suitable for self-prepared prescriptions or self-prepared medicaments.
WO2014011461A1 Amide or urea substituted benzothiazole derivatives as inhibitors of endothelial lipase The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
US20060106072 Compounds having selective activity for Retinoid X Receptors, and means for modulation of processes mediated by Retinoid X Receptors Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.
US7968563 Oxime and hydroxylamine substituted imidazo[4,5-c] ring compounds and methods Imidazo[4,5-c] ring compounds, (e.g. imidazo[4,5-c]pyridines, imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydro imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridine, and 6,7,8,9-tetrahydro imidazo[4,5-c]naphthyridine compounds) having an oxime or hydroxylamine substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
US20080139624 Pellets; sustained release An oral dosage form comprising pellets of a first composition and pellets of a second composition, each composition comprising 5-[4-[2-(N-methyl-N-(2 pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable carrier therefor, wherein the first and second compositions are arranged to release drug at differing release rates on administration, preferably such that the rate of release of the drug from the dosage form is substantially independent of pH; a process for preparing such a dosage form and the use of such a dosage form in medicine.
US20080269259 Regulation of Autophagy and Cell Survival Methods of treating an individual who has been identified as having glycolysis dependent cancer are disclosed. The methods comprise the step of: administering to such an individual a combination of an anti-cancer composition that renders the cancer incapable of glycolysis and an autophagy inhibitor. Pharmaceutical compositions and kits comprising that renders the cancer incapable of glycolysis and an autophagy inhibit are also disclosed. Methods of treating an individual who has a disease characterized b cell degeneration and cell death due to autophagy are disclosed. The methods comprise administering to the individual a permeable form of a metabolic substrate that can be oxidized in the tricarboxylic acid cycle to produce NADH. Methods for identifying an autophagy inhibitor comprising performing a test assay using an apopto sis-resistant cell are disclosed.
WO2011074636A1 Transdermally absorbed preparation of anti-dementia drug Disclosed is a transdermally absorbed prepration that can stably administer an anti-dementia drug over a long period of time on the order of one week. More specifically, the transdermally absorbed preparation of the anti-dementia drug comprises a drug-containing layer comprising the anti-dementia therapeutic drug, a macromolecular compound that has an amino group, a polyvalent alcohol fatty acid ester, a polyvalent alcohol, a polyvalent carboxylate ester, and a styrenic macromolecular compound.
US20100068226 Polynucleotides and Uses Thereof The present invention provides an isolated polynucleotide comprising or consisting of the nucleotide sequence encoding the G protein of human respiratory syncytial virus (RSV), wherein the nucleotide sequence is codon optimised for expression in mammalian cells and wherein the polynucleotide provides increased expression of the G protein in mammalian cells relative to expression of the wildtype RSV-G gene. Preferably, the polynucleotide comprises or consists of the nucleotide sequence of SEQ ID NO:2. Further aspects of the invention provide pharmaceutical compositions, in particular vaccines, for use in methods of immunising a subject against RSV infection.
US20080038307 Biocompatible Coating, Method, and Use of Medical Surfaces The invention relates to medical products having a surface that is at least partially covered by a polymer layer. Said polymer layer is preferably formed by auto-polymerization. Substances containing least one multiple bond, especially unsaturated fatty acids comprising an alkyl chain consisting of preferably between 7 and 50 carbon atoms are polymerized. Other substances which do not participate in the polymerization can be added to the substances participating in the polymerization reaction. Said substances are preferably saturated fatty acids and fatty acid derivatives. The invention also relates to methods for producing such medical products, and to the use of the same.
EP1482939A4 Preparation of paroxetine involving novel intermediates Disclosed are processed for preparing novel carbamate intermediates of paroxetine comprising delakylating N-alkylparoxetine by reaction thereof with a haloalkyl ester of a haloformic acid, in a suitable organic solvent. Also disclosed are processed for preparaing paroxetine comprising hydrolyzing the novel carbamate intermediates in a suitable solvent. Paroxetine prepared by the above processes can be neutralized with hydrogen chloride and crystallized as paroxetine hydrochloride anhydrous, hemilhydrate or as a solvate of isopropanol. The invention is further directed to the novel carbamate intermediates formed by the disclosed processes.
CA2842672A1 Galactooligosaccharides for preventing injury and/or promoting healing of the gastrointestinal tract Disclosed are nutritional compositions including galactooligosaccharides that can be administered to individuals including preterm infants, infants, toddlers, children, and adults for preventing injury and/or improving the healing of the gastrointestinal tract. Additional suitable methods of using the nutritional compositions including the galactooligosaccharides are also disclosed.
EP1735315A1 PYRAZOLO[3,4-b]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS The invention relates to a compound of formula (I) or a salt thereof: formula (I) wherein: R1 is Et, n-Pr, i-Pr, C2fluoroalkyl, or -CH2CH2OH; R2 is H, Me, Et, n-Pr, i-Pr, C1-2fluoroalkyl, cyclopropyl or (cyclopropyl)methyl-; and NHR3 has the sub-formula (nhr3): formula (nhr3) wherein R3a is methyl or ethyl; R3b is H, methyl or ethyl; R3c is H, methyl or ethyl, R3d is H, methyl or ethyl, and R3e is H or methyl, provided that: (a) R3b is methyl or ethyl; and/or (b) R3c and R3d are independently methyl or ethyl; and provided that: (c) when R3c is ethyl and/or when R3d is ethyl and/or when R3e is methyl, then: R3a is methyl and/or R3b is a hydrogen atom (H) or methyl. NHR3 can for example be [(1S)-1,2-dimethylpropyl]amino or t-butylamino. The invention also relates to the use of these pyrazolo[3,4 b]pyridine compounds in therapy, as inhibitors of phosphodiesterase type IV (PDE4), and relates to their use in the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis or allergic rhinitis.
WO2012119605A1 New disperse dye with potent anticancer activity New yellow disperse dye of 2-cinnamyl-5,6,7,8- tetrahydro[l]benzothieno[2,3-d]pyrimidine-4(3H)-one with a first medical application as anticancer showing potent activity against different cancer cell lines and low cytotoxicity to melanocytes (normal skin) which will be helpful in treatment of cancer specially melanoma due to dye stability on the skin.
CN1915235A Application of woodruff acid with acetyl being removed in preparing medicine for treating rheumatoid arthritis An application of the deacetylasperulate in preparing the medicine for treating rheumatoid arthritis is disclosed.
WO2012022121A1 Fused ring compound for use as mineralocorticoid receptor antagonist The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicaments for the treatment and/or prevention of kidney damage, cardiovascular diseases such as hypertension, and/or endocrine diseases. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy, and n are as presented in the description.
US20080119483 Synergistic combination of lipid synthesis inhibitors; no side effects; itraconazole or ketaconazole The present invention provides compositions and methods for inhibiting protozoan growth comprising a synergistic combination of lipid synthesis inhibitors. In addition, the invention provides compositions and methods that are useful for the treatment of protozoan infections and the identification of potential new drugs for the treatment of protozoan infections.
WO2011153221A1 Solid state forms of ixabepilone Crystalline forms of Ixabepilone are described in the present application and processes for preparing the crystalline forms. The present invention also includes pharmaceutical compositions of such crystalline forms of Ixabepilone.
US20090318369 Biomarkers for alzheimer's disease and methods using the same The present invention provides various biomarkers of Alzheimer's Disease (AD). The present invention also provides various methods of using the biomarkers, including methods for diagnosis of AD, methods of determining predisposition to AD, methods of monitoring progression/regression of AD, methods of assessing efficacy of compositions for treating AD, methods of screening compositions for activity in modulating biomarkers of AD, methods of treating AD, as well as other methods based on biomarkers of AD.
EP1814596B1 Antisense antiviral compounds and methods for treating filovirus infection The invention provides antisense antiviral compounds and methods of their use and production in inhibition of growth of viruses of the Filoviridae family, and in the treatment of a viral infection. The compounds and methods relate to the treatment of viral infections in mammals including primates by Ebola and Marburg viruses. The antisense antiviral compounds are substantially uncharged morpholino oligonucleotides having: a) a nuclease resistant backbone, b) 15-40 nucleotide bases, and c) a targeting sequence of at least 15 bases in length that hybridizes to a target region selected from the following: i) the AUG start site region of VP35, as exemplified by antisense compounds SEQ ID NO: 21-26, ii) the AUG start site region of VP24, as exemplified by antisense compound SEQ ID NO:34, iii) the region 85 to 65 base pairs upstream of the AUG start site of VP24, as exemplified by SEQ ID NO:39, iv) the AUG start site region of polymerase L, as exemplified by antisense compound SEQ ID NO: 17, and v) combinations of (i), (ii), (iii), and/or (iv).
CN101381372B Pazufloxacin mesylate and preparation method of powder for injection The invention discloses a method for preparing pazufloxacin mesilate and a powder injection thereof. The method is as follows: a reaction system which is formed by pazufloxacin and methane-sulforic acid as well as a solvent of acetone is subjected to heating and reflux, cooling and crystallization, and separation to obtain the pazufloxacin mesilate, and the pazufloxacin mesilate is then subjectedto aseptic filling and freeze drying to obtain the powder injection of pazufloxacin mesilate. The preparation method of the invention can produce pazufloxacin mesilate for injection which has stable quality.
CN103012417A Carbazole alkaloids in clausena plants, medicine composition with carbazole alkaloids as anti-tumor active component, and preparation method and application of carbazole alkaloids The invention discloses carbazole alkaloids with structural formulas (1-4) of lansine D(1), lansine E(2), lansine F(3) and lansine G(4), a tumor cell growth inhibitor with the carbazole alkaloids as effective components, a preparation method of the carbazole alkaloids, and application of the carbazole alkaloids to the preparation of anti-tumor drugs.
CN101362702A Emodin derivates and application thereof in anti-cancer medicine preparation The invention relates to an emodin derivative and the application in preparing a anti-cancer drug, and the chemical structural formula of the emodin derivative of the invention is as shown in formula I, wherein, R1, R2, R3 are defined as described in the specification; the emodin and the derivative thereon provided by the invention are compounds which are prepared in a way that natural emodin is taken as the matrix, and then structural modification is carried out in accordance with the principles of drug molecules to design out the highly active compounds; experiments proof that the emodin derivative has obvious inhibitory effect on various tumor cells and can be used in preparing cancer-treatment drugs.
WO2014069660A1 Blood flow promoting agent In addition to applications in athletic performance improvement, fat accumulation suppression, and skin quality improvement in connection with the peripheral vasodilatation, this blood flow promoting agent can also be applied to ensuring blood circulation in ischemic diseases, relaxation of blood vessels predisposed to contraction due to age or lifestyle-related diseases, arteriosclerosis prevention, and prevention of shoulder stiffness caused by impaired blood flow, over-sensitivity to cold, erectile dysfunction, thrombosis, etc. This blood flow promoting agent is safe even when dosed over a long period of time, contains, as active components, citrulline or a salt thereof and capsaicin or a capsaicinoid, and in particular exhibits a vasodilating action effective at low doses at which capsaicin does not cause irritation. Also provided are health-promoting foods and functional foods from which the action of this blood flow promoting agent may be obtained.
CN102670644A Process for preparing high-purity medical mirabilite oral liquid The invention discloses a process for preparing high-purity medical mirabilite oral liquid. The process comprises the following steps of: removing mechanical impurities from underground conveyed crude mirabilite water of which the concentration is 9+/-0.5 weight percent (wt%) through a three-stage pipeline filter and a three-stage 1000-mesh titaniferous stainless steel filter screen under the monitoring of a distributed control system (DCS) automatic monitoring system and the regulation of an AK liquid balance flowmeter; performing sixteen-stage ion exchange purification treatment to obtain refined mirabilite water of which the metal ion impurity content is 0.5-1.0ppm; adding blending agents, wherein the volume ratio of dry-basis mirabilite to the blending agents is (8.5-9.5):(0.6-1.5), and the volume ratio of the refined mirabilite water to a flavoring agent is (90-95):(10-5); the blending agents are selected from any four of trichlorosucrose, glucose, sodium cyclamate, magnesium malate, magnesium citrate and sodium benzoate; regulating the mouthfeel of medical mirabilite by any four of the blending agents in mass ratio of 1.0:5.0:5.0:1.0, wherein the flavoring agent is selected from one of lemon essence, apple essence and peach essence; stirring by a high-speed stirring system for 10-30min at the rotate speed of 1500-1800rpm; regulating the pH value to be 7.0+/-0.2; then, delivering into an aseptic packaging system and performing split charging to prepare the high-purity medical mirabilite oral liquid.
WO2013055252A1 Salts of carbamoyl phosphonic acid esters which act as selective inhibitors of human immunodeficiency virus hiv-1 production The invention relates to the field of molecular biology, virology and medicine and concerns novel biologically active compounds, more specifically salts of carbamoyl phosphonic acid esters of the general formula given in the description. The novel compounds are capable of selectively inhibiting the production of human immunodeficiency virus and can therefore be considered for use in the field of medicine for the treatment of AIDS. The compounds are produced by adding an equimolar amount of ammonia, a corresponding amino compound or a hydroxide of an alkali metal or alkaline-earth metal to an acid form of a carbamoyl phosphonic acid ester. The resultant solutions of salts are boiled down to small volumes, from which spontaneous crystallization commences, and are left to stand at 4°С until crystallization ceases, whereupon the precipitates are filtered and dried in a vacuum. The target compound yield is 95-98%. The novel compounds inhibit the proliferation of HIV-1 in MT-4 lymphocyte cell cultures and are stable substances, thus facilitating the creation of drugs based thereon.
CN102327621A Phthalocyanine-serum albumin complex and preparation method and application thereof The invention relates to a phthalocyanine-serum albumin complex and a preparation method and application thereof. The composition consists of a zinc phthalocyanine coordination compound and serum albumin serving as raw materials, wherein the mass concentration ratio of the zinc phthalocyanine coordination compound to the serum albumin is 1-2. The complex can be uniformly dispersed into and exist stably in an aqueous solution, and has good developing prospect. Simultaneously, the preparation method provided by the invention is simple, and the prepared complex is convenient to use, has a remarkable curative effect, is safe and reliable, and has strong killing effects on various cancer cells.
CN103405423A Application of Chukrasone B in medicine for treating renal cancer The invention discloses application of Chukrasone B in preparation of a medicine for treating renal cancer, and belongs to the technical field of new application of medicines. The in-vitro MTT (3-4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) antitumor activity evaluation shows that Chukrasone B has remarkable inhibition effect on the growth of human renal cancer cell line KC, so that Chukrasone B has a good development and application prospect and can be applied to the preparation of the medicine for treating renal cancer. The application of Chukrasone B in the preparation of the medicine for treating renal cancer is disclosed for the first time; the framework type of Chukrasone B is brand new; Chukrasone B brings unexpected inhibition activity for renal cancer cells.
WO2013124340A1 Oral pharmaceutical compositions of dabigatran etexilate Compositions comprising a mixture of at least two types of particles wherein a) the first type of particles comprise dabigatran etexilate in the form of the free base or in the form of pharmaceutically acceptable salts, polymorphs, solvates or hydrates thereof; and b) the second type of particles comprise at least one pharmaceutically acceptable organic acid, use of said compositions in the reduction of the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation and/or in the prevention of venous thromboembolic events in adult patients who have undergone elective total hip replacement surgery or total knee replacement surgery and processes for the preparation of said compositions.
US7601837 Quinoline derivatives and their use as 5-HT6 ligands The present invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.
CN1903203A Application of derivative of polysubstituted acyl thiourea pyrimidine for preparing antiviral medicine An application of polysubstituent acylthiouracil derivative in preparing the antiviral diseases, such as influenza and herpes, is disclosed.
WO2008157302A3 Methods for treatment and prevention of tauopathies and amyloid beta amyloidosis by modulating crf receptor signaling Methods for treating or preventing tauopathies and/or Aβ amyloidosis by modulating CRF receptor signaling. Accumulation of hyperphosphorlyated tau protein in the CNS may be reduced by administration of CRF-Rl selective antagonists and/or CRF-R2 selective agonists. For example, in some aspects, methods for preventing the onset of Alzheimer's disease by administration of CRF-Rl selective antagonist are provided.
US20090118230 Fucose containing proteoglycan or acidic glycan and their pharmaceutical use A class of proteoglycans containing fucosylated acidic glycans, e.g., as produced by marine sponges and sea urchin embryos, have been found to stimulate selective proliferation of mammalian natural killer (NK) cells and γδT cells. These compounds are useful as pharmaceuticals, particularly as immunostimulants, e.g., in the treatment of cancer and viral infections.
US20130059822 Arylfluorophosphate Inhibitors of Intestinal Apical Membrane Sodium/Phosphate Co-Transport The present invention is directed to fluorophosphates, and pharmaceutical compositions thereof, which are inhibitors of intestinal apical sodium/phosphate co-transport and are useful in the treatment of hyperphosphatemia, in reducing blood phosphate levels, and in treating hypertension.
EP1872787A1 Use of defibrotide for the inhibition of heparanase A study has been carried out to verify the effect of Defibrotide on the activity and expression of Heparanase enzyme on myeloma tumor cells (U266) and human microvascular endothelial cells (HMEC). The study has demonstrated that defibrotide can be effectively used for the manufacture of a medicament for the treatment of diseaseses which are positively affected by the inhibition of Heparanse and/or by the downregulation of Heparanse gene expression, such as autoimmune and/or inflammatory diseases.
WO2014087231A3 Pharmaceutical composition having a neuroprotective, nootropic, antiamnesic effect, and method for preventing and/or treating states associated with cerebral circulation disorders, cerebrovascular and neurodegenerative diseases The invention relates to the field of medicine and concerns a pharmaceutical composition based on ethylmethylhydroxypyridine succinate and trimethylhydrazinium propionate, having a neuroprotective, nootropic and antiamnesic effect, and a method for preventing and/or treating states associated with a cerebral circulation disorder, including in the case of a stroke and its after-effects and in the case of cerebrovascular and neurodegenerative diseases or memory disorders, said method including administering a pharmaceutical composition containing ethylmethylhydroxypyridine succinate and trimethylhydrazinium propionate in a therapeutically effective quantity to a patient. The composition has a pronounced synergistic effect, reflected in the considerably improved efficacy of the effect when a combination of ethylmethylhydroxypyridine succinate and trimethylhydrazinium propionate is used in the composition formulation in the case of ischemic damage to the brain, and it reduces fatalities, decreases neurological impairments, and restores memory.
CN103705518A Anti-drug resistant tuberculosis compound targeting bacteria RNA polymerase The invention belongs to the field of pharmacy and relates to an application of a small-molecule inhibitor for mycobacterium tuberculosis, escherichia coli and staphylococcus aureus RNA polymerase and shown by the formula (I) and an application of the compound in preparing a medicine for preventing or treating related bacterial infection diseases. The results of biochemical and biological experiments indicate that the inhibitor shown by the formula (I) has strong adhesion with the target protein, namely, the mycobacterium tuberculosis, escherichia coli and staphylococcus aureus RNA polymerase, and can obviously inhibit the activity of the polymerase and remarkably inhibit the growth of the mycobacterium tuberculosis (including drug-resistant mycobacterium tuberculosis), escherichia coli and staphylococcus aureus. The inhibitor provided by the invention also can be prepared into a disinfectant.
CN102924561A Compound promoting activity of estrogen related receptor alpha (ERR alpha), and its use The invention relates to a compound and its use, and especially relates to a compound promoting the activity of ERR alpha, and its use in the preparation of medicines treating the osteoporosis. The compound can improve the menopausal osteoporosis phenomena.
US20080058399 Candesartan or candesartan cilexetil; improved bioavailability The present invention provides pharmaceutical compositions comprising as an active ingredient candesartan or candesartan cilexetil, compositions exhibiting a relative bioavailability, measured as area under the curve, of more than 1.5.
CN103356998A Composition for treating human white hair and/or leucoderma and application thereof The invention belongs to the fields of medicines, cosmetics and medical appliances, and relates to a composition for treating human white hair and/or leucoderma and an application thereof. The composition contains catalase and L-methionine, wherein the dosage ratio of the catalase to the L-methionine is (50,000-10,000,000U) to (0.01-4g). According to the composition, H2O2-mediated oxidative damages in human hair follicles and leucoderma lesion areas are found as key factors of senile hair bleaching and leucoderma, and not limited by the effect on hair follicle melanocytes. On the basis of the discovery, the composition of taking the catalase and the L-methionine as main effective ingredients is provided; and the composition displays good effects in treatment of the human white hair and the leucoderma.
CN102526041A Application of picrasma quassioides alkaloid serving as STAT3 (Signal Transducer and Activator of Transcription 3) signal specificity inhibitor The invention provides a novel medical application of picrasma quassioides alkaloid, i.e., an application of picrasma quassioides alkaloid serving as a STAT3 (Signal Transducer and Activator of Transcription 3) signal specificity inhibitor. As proved by a cell model screening experiment and Western-Blot detection, the picrasma quassioides alkaloid has high STAT3 inhibiting activity and can be used for effectively inhibiting the expression of relevant genes regulated and controlled by STAT3, so that the growth of tumor cells dependent on STAT3 signals can be inhibited effectively. The picrasma quassioides alkaloid is taken as an active ingredient for preparing an antitumor medicament based on the target spot of STAT3; and antitumor medicaments such as various oral preparations, injections and the like of various dosage forms are prepared from pharmaceutically-acceptable processes and auxiliary materials by taking picrasma quassioides alkaloid as an active ingredient.
US20120070411 Substituted nucleotide analogs Disclosed herein are phosphoroamidate nucleotide analogs, methods of synthesizing phosphoroamidate nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the phosphoroamidate nucleotide analogs.
US20110301241 New halo active aromatic sulfonamide organic compounds and uses therefor Aromatic N-halosulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to release active halogen ions has been utilized in a range of biocidal and fungicidal applications. This disclosure deals with the use of halo active aromatic sulfonamide organic compounds as odor control and/or biocidal agents in a cleaning solution for use with bovines and other dairy animals.
US7423012 Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.
CN101084911B Notoginsenoside sodium freezing-dried emulsion and preparation method thereof An escin sodium lyophilization dry emulsion for injection comprises therapeutically-effective amount of escin sodium and carrier material comprising phospholipid, emulsifying agent, water-soluble adjuvant and freeze-dried stabilizer. Its preparation method comprises preparing escin sodium into internal water phase, adding organic phase containing phospholipid, preparing into colostrum, adding outer water phase, preparing into emulsion of w/o/w, adding freeze-dry protective agent, and freeze-drying into solid.Berore application, water for injection is added as required for hydration, and oscillating, and emulsion is otbtained after recovery. The escin sodium lyophilization dry emulsion for injection has the advantages of reduced stimulatory function, increased toleration of clinical application and stability of medicament due to the protection of water-soluble stabilizer in adjuvant and phospholipid, thereby avoiding direct contact of lyophilization dry emulsion with wall of blood vessel.
US20120308568 Pharmaceutical composition for inhibiting abnormal proliferation of cells The present invention relates to a pharmaceutical composition for preventing or treating diseases related to abnormal proliferation of cells, comprising a cytoplasmic heat shock protein (Hsp)60 kDa inhibitor as an active ingredient, and to a screening method and a kit using the composition. According to the present invention, substances which inhibit expression of cytoplasmic Hsp 60 genes or inhibit activity of cytoplasmic Hsp 60 or inhibit binding between cytoplasmic Hsp 60 and IKK protein prevent interaction between cytoplasmic Hsp 60 and IKK complexes to make NF-κB path inactive, and thus induce apoptosis. Therefore, the substances can be valuably used in preventing or treating diseases related to abnormal proliferation of cells, such as cancer, inflammatory diseases or hyperproliferative vascular diseases.
CN103169762A Drug for enhancing immunity of animals The invention discloses a drug for enhancing the immunity of animals. The drug comprises the following components by weight percent: 40-50% of echinacea, 10-15% of herba epimedii, 10-20% of gensing, 20-30% of bee glue, 10-15% of mongolian oak peel, 10-15% of liquorice, 5-10% of honeysuckle and 5-10% of ceftiofur sodium. The drug can be independently and orally taken or used as a feed additive and is low in production cost, good in stability and suitable for industrial production. Proved by clinical experiments, the drug can be used for effectively enhancing the immunity of a human body, remarkably reducing various bacteria and the morbidity of viral diseases and being matched with other drugs to treat various animal diseases. The invention also discloses a preparation method of an oral liquid of the drug for enhancing the immunity of the animals.
WO2009029439A1 Substituted piperazinyl pyrazines and pyridines as 5-ht7 receptor antagonists The present invention provides selective 5-HT7 receptor antagonist compounds of Formula (I) and their use in the treatment of migraine: where A is C(H)= or N=; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyridyl, or thienyl; R2 is hydrogen or methyl; and R3 and R4 are as defined herein.
WO2008146919A1 Lincosamide derivative, and antibacterial agent comprising the same as active ingredient Disclosed is a compound represented by the formula (I) or a pharmacologically acceptable salt or solvate thereof [in the formula (I), A represents an aryl group and R1 represents a 5- or 6-membered monocyclic heterocyclic group, or A represents a 4- to 6-membered monocyclic heterocyclic group and R1 represents an aryl group or 5- or 6-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or a C1-6 alkyl group; R3 represents a C1-6 alkyl group or a (C3-6 cycloalkyl)-(C1-4 alkyl) group; R4, R5 and R6 independently represent a hydrogen atom; R7 represents a C1-6 alkyl group; and m represents a number of 1 to 3]. The compound is a novel lincosamide derivative having a potent activity against a drug-resistant Streptococcus pneumoniae bacterium. The compound can be used as an antibacterial ingredient, and is useful for the prevention or treatment of a bacterium-mediated infectious disease.
US20110152245 Substituted benzamides The invention relates to compounds of formula wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
US20100034813 Substituted pyrazole and triazole compounds as ksp inhibitors Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:
EP1377577B1 Pyrrole derivates for treating cytokine mediated diseases Compounds of formula (I): [wherein: A is a pyrrole ring; R1 is an optionally substituted aryl or heteroaryl group; R2 is an optionally substituted nitrogen-containing heteroaryl group; and R3 is formulae (IIa), (IIb) or (IIc), wherein m is 1 or 2, one of D and E is nitrogen and the other is ⊃C(R5)- (wherein R5 is hydrogen, a Substituent ≡ or a Substituent β), B is a nitrogen-containing 4- to 7-membered heterocyclic ring, and R4 is from 1 to 3 substituents from Substituent group ≡, substituent group β and Substituent group η; PROVIDED THAT R?1 and R3¿ are bonded to the two atoms of said pyrrole ring which are adjacent to the atom of the pyrrole ring to which said substituent R2 is bonded; Substituent group ≡ consists of hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio and halogeno alkythio groups and groups of formula NRaRb (wherein R?a and Rb¿ are hydrogen, alkyl, alkenyl, alkynyl, aralkyl and alkylsulfonyl, or R?a and Rb¿, taken together with the nitrogen atom to which they are attached, form a heterocyclyl); Substituent group β consists of optionally substituted alkyl, alkenyl and alkynyl groups, and aralkyl and cycloalkyl groups; Substituents group η consists of oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsufinyl, alkylsulfonyl, optionally substituted aryl, optionally substituted aryloxy, alkylidenyl and aralkylidenyl groups] have excellent activity against the production of inflammatory cytokines.
CN1820746A Stepronin powder injection and its preparing method The present invention is new preparation form of Stepronin, especially Stepronin powder for injection, and its preparation process. The powder for injection consists of Stepronin or its metal salt or amino salt as active component and freeze drying support agent. Compared with available orally taken Stepronin preparation, the present invention has the advantages of high bioavailability, good medicine absorption, fast medicine dispersion, fast acting, etc. The present invention expands the administration range of Stepronin and raises the clinical administration level of Stepronin.
EP2231652B1 Novel 2-hetaryl thiazole-4-carboxamide derivatives, production thereof, and use thereof as a medicament The invention relates to 2-hetaryl thiazole-4-carboxamide derivatives of formula (I), the use thereof as a medicament for treating various diseases, and methods for the production thereof.
CN101596318A External preparation for treating androgens psilosis, seborrheic dermatitis and acne The invention provides an external prescription and a preparation process of a 5alpha-reductase inhibitor external preparation for treating androgen spsilosis , seborrheic dermatitis and acne (common comedo). In the prescription and the preparation process, a 5alpha-reductase inhibitor is used as a main medicine and a diluent antiseptic agent, a dissolve-helping moisturizing antiseptic agent, a dissolve-helping disinfecting agent, a softening percutaneous absorption promoter, an antiseptic disinfecting agent, diluent agent, and the like as auxiliary materials, wherein the 5alpha-reductase inhibitor which is originally and orally taken is prepared into an external solution to be directly applied on wounded parts so as to effectively treat the spsilosis, the seborrheic dermatitis and the acne and also reduce side effect caused in such a way that the 5alpha-reductase inhibitor is orally taken to treat the spsilosis. The invention has simple preparation process and good stability.
WO2006104153A1 Composition for increasing anti-oxidation activity in blood Disclosed is a composition which serves to maintain a high level of reduced coenzyme Q10 in the blood upon intake of the coenzyme Q10 even in an elderly mammal to thereby maintain a high level of anti-oxidation activity in the blood. A composition for increasing the anti-oxidation activity in the blood in an elderly mammal, the composition comprising reduced coenzyme Q10 as the active ingredient.
US20120238555 Pharmaceutical composition containing irbesartan This invention relates to pharmaceutical compositions containing irbesartan, providing oral formulations with a high relative amount or concentration of irbesartan. In one embodiment, the present invention provides an oral formulation of irbesartan containing greater than 70% w/w irbesartan. In another embodiment, the invention provides an oral formulation of irbesartan which exhibits a dissolution profile according to which greater than about 85% of the Irbesartan is dissolved within about 30 minutes using USP apparatus 2, placing the tablet in 1000 mL of 0.1N hydrochloric acid at 37° C. with paddle speed of 50 rpm. The formulation can optionally contain at least one additional active ingredient.
US7084160 2-Amino-(imidazole, thiazole, or oxazole) derivatives; tyrosine kinase, endothelial growth factor, angiogenesis and fibroblast growth factor inhibitors; anticarcinogenic and antidiabetic agents The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
CN103655613A Application of arsenic trioxide and water-soluble object thereof in preparing medicine for treating pancreatic cancer The invention belongs to the field of medicine pharmacy, and in particular relates to application of arsenic trioxide and a water-soluble object thereof arsenious acid serving as an SHH (sonic hedgehog) signal pathway inhibitor in preparing a medicine for treating pancreatic cancer. By virtue of animal experiments, arsenic trioxide and combined administration are applied to intervention of a nude mouse with human pancreatic carcinoma cell line transplanted tumor, and results indicate that arsenic trioxide has a remarkable growth inhibition effect to the occurrence of pancreatic carcinoma transplanted tumor and can lower the expression of SHH terminal member GL11 protein and target gene thereof of the pancreatic carcinoma cell line transplanted tumor and the expression of related indexes ALDH, CD24 and CD44 of tumor stem cells, and indicate that arsenic trioxide plays the effect of an SHH signal pathway inhibitor in an animal body and enables the GLI protein to lose activity. The arsenic trioxide and the water-soluble object thereof can be used as the SHH signal pathway inhibitor for preparing a medicine for treating pancreatic cancer.
CN103040871A Acne therapeutic agent and preparation method thereof The invention discloses an acne therapeutic agent and a preparation method thereof. The acne therapeutic agent comprises the following components by weight parts: 20-40 parts of polyoxyethylene sorbitol monolaurate, 10-20 parts of mineral oil, 3-6 parts of dodecyl dimethyl amine oxide, 1-3 parts of hydroxyl propyl methyl cellulose, 4-8 parts of Vaseline, 1-3 parts of erythromycine, 3-5 parts of pearl powder, 10-20 parts of propylene glycol, 10-16 parts of glyceryl monostearate, 0.1-0.3 part of essence and 80-100 parts of distilled water. Compared with the prior art, the acne therapeutic agent has the benefits that: (1), the curative effect is obvious, the cure rate is more than 95 percent, and no side effect is generated; and (2), the functions of resisting bacterium, relieving itching and solving cuticles of pores are achieved.
US7635464 Selective targeting of apoptotic cells The invention relates to a method of selectively targeting an active agent (or agent capable of becoming an active agent) to apoptotic cells in a vertebrate, comprising administering to said vertebrate a system comprising an arsenoxide (or arsenoxide equivalent) compound and said agent, wherein said system selectively targets apoptotic cells.
US20080221058 Tumor-Specific Vector for Gene Therapy The invention relates to a vector for the gene therapeutic treatment of tumors, especially in connection with radiotherapy. Said vector is provided with a therapeutic gene in the DNA sequence thereof. The gene is controlled by the promoter for the catalytic subunit of the telomerase or by the promoter for cyclin A.
US20120058086 Compositions, kits, and methods for promoting ischemic and diabetic wound healing Compositions, kits and methods for promoting diabetic wound healing are based on the discovery that SDF-1α specifically upregulates expression of E-selectin in mature endothelial cells (EC), leading to an increase in EC-endothelial progenitor cell (EPC) adhesion and EPC homing. Methods for promoting healing of a wound in a diabetic subject include providing a therapeutically effective amount of a composition including E-selectin protein or a nucleic acid encoding E-selectin protein, and optionally, an agent that specifically upregulates E-selectin expression (e.g., SDF-1α). The methods can also include administering hyperbaric oxygen treatment to the subject. Administering the composition to the subject results in migration of bone marrow-derived progenitor cells to the wound, accelerated wound healing, and upregulation of E-selectin expression in the subject.
US20080132455 Process For Producing Enriched Fractions Containing Up To 100% Of Bacopasaponins From The Plant Materials Of Bacopa Species This invention describes a process for producing a fraction enriched with jujubogenin and psudojujubogenin lycosides from Bacopa species, wherein the total Bacopa saponin concentration is up to 100% when estimated by HPLC method of analysis. The present invention also describes the processes for the enrichment of new compositions and individual saponin compounds from Bacopa munnieri to more than 95% purity. It further describes an analytical HPLC method for the estimation of total Bacopa saponin fraction and its use in therapeutic applications. This invention also includes two Bacopa saponin 3-O-[β-D-glucopyranosyl-(1 3)-β-D-glucopyranosyl] jujubogenin and 3-O-[β-D-glucopyranosyl-(1 3)-β-D-glucopyranosyl] pseudojujubogenin herein referred to as bacopaside N1 of general formula (1) and bacopaside N2 of general formula (2) respectively.
WO2013123588A9 Co-use of a clusterin inhibitor with an egfr inhibitor to treat cancer Epidermal growth factor receptor (EGFR) expression and phosphorylation is increased in cancer cells treated with anti-clusterin antibodies. Such treatment is also accompanied with the reappearance of an epithelial phenotype of the cancer cell, as determined by an increased E-cadherin expression at the surface of cancer cells. Clusterin inhibitors may thus induce reversal of the epithelial to mesenchymal phenotype and restore sensitivity of cancer cells to EGFR inhibitors. Combinations of a clusterin inhibitor and an EGFR as well as their use in treatment of cancer are thus provided herewith.
US20110086087 Process and Formulation for Immunizing Fish in Aquaculture Systems Process, use, method and formulation of inclusion of Deoxyribonucleic acid (DNA) in food compositions for livestock animals, in particular in aquacultural systems.
WO2008019276A2 Solid forms of (3'-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl)methanone and methods of their use Solid amorphous and crystalline forms of (3'-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl)methanone are disclosed, in addition to methods of their use in the treatment of various diseases and disorders.
CN101292966A Solid dispersion of resveratrol and glycosides and preparation method thereof The invention discloses a solid dispersion of resveratrol and glucoside and the preparation method thereof. The resveratrol and glucoside comprise one of the resveratrol and piceid or the mixture thereof, belonging to the fields of drugs and health care products. The solid dispersion is composed of the following raw materials by weight proportions: resveratrol or piceid: carrier: additive equals to 1:1-20:0-10. The invention adopts a melting method and a solvent method to prepare the solid dispersion of resveratrol and glucoside, and the solid dispersion is cause to have good water-solubility or water dispersivity and can be fabricated into wine or fruit juice of strengthened resveratrol.
CN102451288A Special medicinal preparation for preventing and treating beriberi The invention provides a special medicinal preparation for preventing and treating beriberi. The medicinal preparation is prepared from a component A and a component B, wherein the component A comprises, by weight, 5-12 parts of Fructus Anisi Stellati, 1-12 parts of Solanum nigrum L., 5-15 parts of Saxifraga stolonifera Curt., 3-10 parts of Wrinkled Gianthyssop, 5-15 parts of willow leaf and 5-10 parts of Fructus Cnidii; and the component B comprises, by weight, 6-15 parts of borneol, 2-16 parts of salicylic acid, 25-35 parts of safflower, 0.5-3 parts of tannic acid and 0.5-1.5 parts of furacilin. The medicinal preparation which is suitable for sweat prevention and foot comfort, beriberi and foot odor eradication, ringworm removal and itching relief, and skin protection has the advantages of reasonable formula, substantial usage effect, small restriction, difficult recurrence after the usage, no toxic side effect, sterilization and bacteriostasis, difficult anaphylactic reaction generation, and safety and reliability.
US20120264708 Method For Treatment Of Macular Degeneration By Modulating P2Y12 or P2X7 Receptors Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and/or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and/or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.
EP1509231B1 System for peritoneal dialysis comprising a reservoir of dialysis solution and a cartridge containing taurolidine powder The present invention contemplates the addition of 0.5% to 4% taurolidine into solutions used peritoneal dialysis. The taurolidine is intended to prevent or reduce the incidence of infection within the abdomen and/or in the vicinity of an implanted dialysis port. The invention also includes methods using solutions of taurolidine in the flushing and locking of catheters and fluid lines used in peritoneal dialysis.
US7368144 Removal of shell, pulp; grinding in presence of solvent; macerating, extraction. filtration The invention concerns a method for obtaining extracts based on polyphenol compounds contained in cocoa, characterised in that it includes: using fresh beans, which have not been pre-treated or defatted, said fresh beans whereof their pulp and shell have been eliminated, so as to obtain clean almonds; grinding said almonds, in the presence of solvent(s); macerating the ground almonds in conditions enabling extraction of the desired compounds; filtering the macerated mixture; recuperating an extract containing said compounds from the filtrate. The invention also concerns the extracts and their uses for cosmetic, food and therapeutic purposes.
CN103040822A Drug composition containing kurarinone compound and preparation method of drug composition The invention provides a drug composition containing a kurarinone compound and a preparation method of the drug composition. The drug composition comprises kurarinone and vitamin B6. Researches find that the kurarinone and the vitamin B6 have a certain synergistic effect in treating leukopenia, and the dosage of the kurarinone can be reduced. The drug composition can be prepared into an injection or a powder injection. According to the drug composition and the preparation method, mannitol, edetate disodium and dextran are collocated reasonably to be prepared into freeze-dried powder, the stability of the preparation can be improved, the dosage of mannitol and dextran can be reduced, and the drug composition is good in freezing type and appearance.
CN103623419A Chlorotoxin-targeted oxidized graphene nanometer material used for transporting antitumor drug A method for preparing a CTX (Chlorotoxin)-targeted oxidized graphene nanometer material comprises the following steps: 1, mixing graphite and H2SO4-HClO4, stirring and mixing the mixture in an ice-bath, continuing stirring in a warm water bath , heating to 100 to 120 DEG C for deacidification, diluting to 800 to 1000 ml and then centrifuging, adding an alkali solution and then mixing and settling, stirring at 70 to 90 DEG C and filtering under the condition of being hot, washing to be approximately neutral, and freeze drying at minus 40 DEG C under the vacuum condition to obtain oxidized graphene; 2, mixing the oxidized graphene with a phosphate buffer solution, adding N-Hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride to perform an activating reaction at room temperature; adjusting the pH value of the mixture to be 7.0 to 8.0, adding CTX for reaction, centrifugating and washing the obtained product, and performing vacuum freeze drying at minus 40 DEG C to obtain the CTX-targeted oxidized graphene nanometer material. The material can be used for transporting an anticancer drug of adriamycin to a brain glioma in a targeted manner.
WO2013149581A1 Combination products with tyrosine kinase inhibitors and their use The present invention relates to pharmaceutical products comprising a combination of (i) a MET inhibitor and (ii) an EGFR inhibitor, or a pharmaceutically acceptable salt thereof, respectively, or a prodrug thereof, which are jointly active in the treatment of proliferative diseases, corres- ponding pharmaceutical formulations, uses, methods, processes, commercial packages and related invention embodiments.
WO2008017206A1 A percutaneous intratumoral injection composition for treating thyroma A percutaneous intratumoral injection composition for treating thyroma. It comprises greater than 50wt% of ethanol, less than 10wt% of active ingredient of Chelidonium majus L., and the pH value of said composition does not fall within the range of 7.35-7.45.
US20090123529 Nucleic acid immunological composition for human metapneumovirus There is provided an immunological composition that comprises a nucleic acid vector which includes a promoter region operably linked to a coding sequence encoding the human metapneumovirus F antigen or the human metapneumovirus G antigen. The immunological composition is useful for administering to an individual to elicit an immune response to human metapneumovirus in the individual and for the generation of diagnostic reagents for hMPV.
US20100004306 PIGF-1 Assay and kits and components thereof The present disclosure relates to, among other things, methods for determining whether a subject receiving treatment with a drug has obtained an efficacious blood level of the drug. Moreover, the present disclosure also relates to methods of determining whether a subject predisposed to or suffering from a disease will benefit from treatment with a drug, and the response of a subject receiving treatment (e.g., such as for cancer) by monitoring biomarkers of angiogenesis. In particular, the disclosure relates to PlGF-1 companion diagnostic methods and products.
CN101204202B Ruminant granular humic acid feed The invention belongs to the technology field of animal husbandry and is a new feedstuff for ruminants, which is characterized by low cost, safe feeding and growth promoting. Based on the nutritional requirements of ruminants and combined with the present production condition, the invention initially develops non-conventional feedstuff resources to provide humic acid granulated feedstuff by taking full advantage of humic acid resources of an open cola mine. The production of the invention is characterized by safety and effectivity, low cost and capacity of improving the immune and disease-resistance abilities of animal bodies. The invention also plays a significant role in promoting the development of ruminant breeding industry.
WO2009132453A8 Cyclylamine derivatives as calcium channel blockers Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted cyclylamine derivatives as shown in formulas (1).
WO2004062610A3 4',4''-SUBSTITUTED 3α-(DIPHENYLMETHOXY)TROPANE ANALOGS FOR TREATMENT OF MENTAL DISORDERS The present invention describes a method for the treatment of attention deficit hyperactivity disorder (ADHD), conduct disorder, alcohol addiction, tobacco addiction, nicotine addiction, parkinsonim including Parkinson's disease, female and male orgasmic disorders, female and male sexual arousal disorders, hypoactive sexual desire disorder, and disorders characterized by anxiety and/or depression. In this method, a therapeutically effective, nontoxid dose of a 4',4''-substituted 3α-(diphenylmethoxy)tropane analog or a pharmaceutically acceptable salt thereof is administered to the patient in need of such treatment.
EP1954274A2 Substituted quinolones and methods of use Substituted quinolone compounds and compositions are provided along with methods for the use of those compounds in the treatment of diseases and disorders such as cancer.
EP1507537A1 Combination of an ace inhibitor, a calcium channel blocker and a diuretic The present invention relates to a method of treatment of a condition or disease selected from the group consisting of hypertension, left ventricular dysfunction and hypertrophic cardiomyopathy, diabetic cardiac myopahty, supraventricular and ventricular arrhythmias, atrial fibrillation, atrial flutter, detrimental vascular remodeling, myocardial infarction and its sequelae, antheroscleorosis, angina (whether unstable or stable), renal insufficiency (diabetic and non-diabetic), heart failure, angina pectoris, diabetes, secondary aldosteronism, primary and secondary pulmonary hypertension, renal failure conditions, such as diabetic nephropathy, glomerulonephritis, scleroderma, glomecular sclerosis, proteinuria of primary renal disease,and also renal vascular hypertension, diabetic retinophathy, the management of other vascular disorders, such as migraine, peripheral vascular disease, Raynaud´s disease, luminal hyperplasia, endothelial dysfunction, cognitive dysfunction( such as Alzheimer's), glaucoma and stroke, comprising administering, to a mammal in need thereof, a therapeutically effective amount of a combination comprising (i) an ACE inhibitor, (ii) a calcium channel blocker (CCB), and (iii) a diuretic.
EP1616861A2 A process for the preparation of keto compounds A process for the preparation of 4-[1-oxo-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-α,α-dimethylbenzeneacetic acid, useful as an intermediate in the preparation of fexofenadine.
CN102993197A Tropinone derivative, and preparation method and application thereof The invention belongs to the preparation field of a new compound, and particularly relates to a tropinone derivative, and a preparation method and an application of the tropinone derivative. The tropinone derivative and pharmaceutically acceptable salt of the tropinone derivative have the structural formula shown by a general formula I, wherein R2 is selected from alkyl group with 1-6 carbon atoms, aromatic group with 1-20 carbon atoms, heterocyclic ring with 1-20 carbon atoms, and amino group; X is selected from alkyl group with 1-6 carbon atoms, aromatic group with 1-20 carbon atoms, heterocyclic ring with 1-20 carbon atoms, methylsulfonyl and p-tosyl; or R1 is selected from alkyl group with 1-6 carbon atoms, aromatic group with 1-20 carbon atoms, and heterocyclic ring with 1-20 carbon atoms. The tropinone derivative can be used for preparing a medicine for treating II type diabetes mellitus.
CN103554140A Preparation method and application of anthraquinone polypyridine ligand and binuclear ruthenium complexes The invention discloses a novel anthraquinone polypyridine ligand and a preparation method thereof. The anthraquinone polypyridine ligand is simple in synthetic method and can be further used for preparing binuclear ruthenium complexes. The prepared anthraquinone polypyridine binuclear ruthenium complexes as shown in a general formula of [(bpy) 2Ru (X-biipad) Ru (bpy) 2] (ClO4)4 have the advantages of stable structure and high water solubility, can effectively inhibit the migration of tumor cells and cell invasion according to the results of cell wound scratch assay and cell invasion assay, and can be used for preparing novel antineoplastic drugs for inhibiting tumor metastasis.
US20050080141 Amino diols useful in the treatment of alzheimer's disease The present invention relates to the treatment of Alzheimer's disease and other similar diseases, and more specifically to the use of compounds that inhibit beta-secretase, an enzyme that cleaves amyloid precursor protein to produce A beta peptide, a major component of the amyloid plaques found in the brains of Alzheimer's sufferers, in such methods.
EP2636406A1 Ibuprofen Intravenous Infusion The present invention is a novel pharmaceutical formulation that compromises a four mg per ml (4 mg/mL) Ibuprofen in an aqueous solution of Arginine and Ibuprofen, wherein the molar ratio of Arginine to ibuprofen is more than or equal to 1.000625:1, Tris buffered, isotonic, and adjusted to pH between 7.2- 8.5 by addition of 1.0 N HCL, none of the excipients used contains material of animal or human origin. There were no novel excipients used. The present invention also provides a method of treating through anti-inflammatory, analgesic, and antipyretic activity: fever, pain, dysmenorrhea and inflammatory diseases such as rheumatoid arthritis and muscles. It is also used for pericarditis and patent ductus arteriosus (Patent ductus arteriosus (PDA)), relieve moderate to severe pain, dental pain and pain after an operation, also relieve mild to moderate pain including migraine headache, as well as for short term treatment of pyrexia in children over one year of age. The formulation is meant to be used as ready to use intravenous infusion.
US8003789 Activity against strains having acquired resistance nonnucleoside reverse transcriptase inhibitors; human alpha1 acid glycoprotein nonbinding; such as 4-[[(5-bromo-4,6-dichloro)-2-pyrimidinyl]amino]-benzonitrile This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, 13 NHC(═O)R6,—C(═NH)R6, aryl; for the treatment of subjects suffering from HIV infection.
US20080114016 5-(3-aminopropyl)-3-methyl-2,5,7,8,9,10-hexahydro-4H-benzo[g]pyrazolo[4,3-c]quinolin-4-one; anticarcinogenic agent; enhance DNA damaging agents by initiating mitosis before DNA repair is complete and thereby causing tumor cell death; in preparation of a anticancer medicaments The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by ad-ministering the compound to a patient in need of treatment of cancer.
CN101210014A Setron-like compounds, preparation method and medicament use thereof The invention provides a new steron compound and a preparation method thereof; furthermore, the invention also relates to salt containing the compound or salt acceptable in pharmacy and usage used for preparing 5- hydroxytryptamine 3 receptor antagonist medicines. The steron compound of the invention or the salt acceptable in the pharmacy is the 5- hydroxytryptamine 3 receptor antagonist preparation of active constituent, which can treat nausea and vomiting symptoms of cancer patients caused by chemo-treatment.
EP1307594A4 Association of sim2 with cancer Disclosed are methods of detecting cancer in a biological sample by detecting SIM2 nucleic acid or protein in the sample. Also disclosed are methods for treating cancer and identifying compounds that modulate SIM2 expression.
EP1200108B1 Use of ginkgo extract for treating cancer which is characterized by an over-expression of peripheral-type benzodiazepine receptor protein The present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated Ginkgolide B (GKB), a component of the extract of Ginkgo biloba leaves in a method for decreasing the expression of peripheral-type benzodiazepine receptor (PBR) in cells of a patient in need thereof. Further, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in a method for decreasing the proliferation of cancer cells in a patient. More particularly, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in a method of decreasing cancer cell proliferation in a patient wherein the cancer cell is human breast cancer cell. Even more particularly, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in method of decreasing cancer cell proliferation in a patient wherein the cancer cell is of the aggressive and invasive phenotype and expresses high levels of PBR in comparison to non-aggressive cancer cell.
CN101249136A Applications of compound red sage root tablet for pharmacy The invention relates to a new application of a compound salvia tablet in the pharmaceutical field. The compound salvia tablet has the effect of preventing the complication induced by high-level glycosylated hemoglobin through inhibiting the generation of the glycosylated hemoglobin; the compound salvia tablet can be used for preparing drugs which are used for preventing and inhibiting the generation of the diabetes mellitus glycosylated hemoglobin and treating the chronic complications induced by the diabetes mellitus glycosylated hemoglobin, wherein, the chronic complications comprise retinopathy, cataract, atherosclerosis, myocardial infarction, cerebrovascular disorder, heart failure, periodontitis and osteoporosis; the compound salvia tablet can improve the 2 diabetic insulin resistance and inhibit the development of the diabetes mellitus and the generation of the complication. The new application has the advantages that the compound salvia tablet is a Chinese patent drug with long history and definite curative effect, the side-effect is less, the resources are rich, the fabrication technology is simple, and the quality is stable and controllable; the compound salvia tablet can be used for preparing the drugs which are used for preventing or treating the chronic complications induced by the diabetes mellitus glycosylated hemoglobin; the market prospect is very broad.
WO2009027349A3 Treatment and prevention of neurodegenerative diseases The treatment and prevention of neurodegenerative diseases by repression of the transcriptional complex that silences the promoter of the UCHL1 gene.
WO2007048918A1 Novel esterified amino compounds having a hydrocarbon ring e with six camptothecin analogue ring members, preparation method thereof and pharmaceutical compositions containing same The invention relates to a compound having formula (I), wherein: R1, R2, R3, R4, R5, R70, R80, R90, R71, R81, R91, Alk, Alk', X, X' and G are as defined in the description. The invention also relates to medicaments containing same.
CN1895389A Liver-nourishing beverage A liver-nourishing beverage is prepared from purified water and 8 Chinese-medicinal materials including reagle, barbat skullcap, frankincense, peach kernel, etc.
CA2834422A1 Method for utilizing extraction residue of yeast extract [Problem] To produce a glycosylceramide composition which is suitable for a functional food, a medicinal product and the like and has stable quality, and from which contaminants such as sterol glycosides are removed, specifically to produce the glycosylceramide composition at low cost using a material that has been eaten by human beings, is safe and is readily available as a raw material. [Solution] An yeast residue that is produced as the result of the extraction of an yeast extract from Torula yeast or the like is used as a raw material, and the yeast residue is extracted with an organic solvent such as an alcohol, thereby producing a glycosylceramide-containing composition.
US20100197766 Antisense Oligonucleotides Directed to Ribonucleotide Reductase R2 and Uses Thereof in the Treatment of Cancer The present invention provides antisense oligonucleotides directed to a mammalian ribonucleotide reductase R2 gene and combinations of the antisense oligonucleotides with one or more chemotherapeutic agents for use in the treatment of cancer.
WO2004016764A3 eNOS MUTANTS USEFUL FOR GENE THERAPY The present invention provides endothelial nitric oxide synthase (eNOS) polypeptide mutants and polynucleotides encoding such polypeptide mutants, useful for gene therapy. In particular, the invention provides eNOS polypeptide mutants having one or more mutations in an amino acid sequence corresponding to a functional domain of a mammalian eNOS. More particularly, the invention provides eNOS polypeptide mutants having at least one mutation at a position corresponding to an amino acid residue in a calmodulin-binding site that is phosporylated in mammalian cells, where the mutation is not an amino acid substitution to Ala or Asp in an eNOS polypeptide mutant having a single mutation that is at the phosphorylation site ; and to polynucleotides encoding such polypeptide mutants. The present invention further provides prophylactic, diagnostic, and therapeutic methods of using such eNOS polypeptide mutants and polynucleotides.
WO2009088997A1 Lactam inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell. (I)
WO2013033862A1 4-substituted-(3-substituted-1h-pyrazole-5-amino)-pyrimidine derivatives having activity of inhibiting protein kinase and use thereof Provided are derivates substituted with urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation method and use the compounds.
CN1857368A Medicine composition for treating diabetes The present invention belongs to the field of medicine technology, and especially a kind of diabetes treating medicine composition and its preparation process and use. Specifically, the medicine composition is prepared with glibenclamide, puerarin, trichosanthes root and taurine. The medicine composition has high curative effect on diabetes and can lower the incidence rate of diabetes complication, including diabetic nephropathy, and its taurine can reduce the angle of repose of the medicine composition powder to smaller than 30 deg and improve the flowability of medicine composition powder.
CN102600199A Methods for increasing cytidine levels in vivo and treating cytidine-dependent human diseases The present invention is directed to methods of improving cognitive and neurological functions and increasing synthesis and release of neurotransmitters and membrane synthesis by neural cells and brain cells, comprising administering a composition comprising a uridine.
US20050020482 Methods for modulating gap junctions A method for modulating gap junctions is provided. In a first step, the transcription of connexin is enhanced and the gap junction is relocalized at the cell membrane; in a second step, gap junction function is restored by properly gating the channel and/or inducing apoptosis. The method preferably comprises a providing a cell or an animal with a first compound for increasing the activity of protein kinase A (PKA) and in the second step providing the cell or animal with a second compound for specifically inhibiting or activating one or more protein kinase C (PKC) isoforms and/or for specifically inhibiting p38 MAP kinase.
WO2008050600A1 Therapeutic or preventive agent for intractable disease based on oxidative stress-mediated cell death as molecular background A therapeutic or preventive agent for an intractable disease based on oxidative stress-mediated cell death as a molecular background according to the invention contains a compound represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient. (1) In the formula, R1 represents a hydrogen atom, R2 represents a C6-C10 aryl group which may have a C1-C3 alkyl group as a substituent; or R1 and R2 may be combined with each other to form a tetrahydrofuranyl ring together with the adjacent oxygen atom; and R3 and R4 are independent of each other and represent a hydrogen atom, a pyridyl group or a C6-C10 aryl-C1-C3 alkyl group which may have a halogen atom as a substituent.
US20120059013 Method of treating early morning akinesia in subjects having parkinson's disease The present invention provides a method for treating early morning akinesia, comprising continuous administration to a patient in need of such treatment a therapeutically effective amount of a dopamine agonist or a pharmaceutically acceptable salt, enantiomer, solvate, hydrate, polymorph or prodrug thereof.
WO2012033189A1 Agent for treatment of dry eye characterized by combining p2y2 receptor agonist with hyaluronic acid or salt thereof, method for treating dry eye, and use of the p2y2 receptor agonist and hyaluronic acid or salt thereof Disclosed is an agent for the treatment of dry eye, which is characterized by combining a P2Y2 receptor agonist at a therapeutically effective concentration with hyaluronic acid or a salt thereof at a therapeutically effective concentration. This agent for the treatment of dry eye, which is in the form of an ophthalmic agent, remarkably promotes tear secretion and remarkably improves corneal epithelial disorder, and is thus expected to be a novel agent for the treatment of dry eye.
CN1939316A Microsphere containing adriamycin, its usage and preparation A doxorubicin microball used for arterial embolism, intratumor injection, tumor-side injection, or lumbar injection is prepared from polylactic acid-hydroxyacetic acid copolymer. Its preparing process is also disclosed.
CN1872058A Medication composition of containing macrolides A composite medicine with higher biologic utilization rate contains the microemulsified and pre-concentrated solutions of macrocyclic lactone compound, 1,2-propanediol, hydrophilic surfactant, and medium-and long-chain saturated or unsaturated lipophilic glyceride of fatty acid.
WO2013117713A1 Reversal of senescence The present invention relates to the reversal of senescence, in particular the reversal of p16-mediated replicative senescence, using p16 inhibitors. The p16 inhibitors are generally small interfering RNA (siRNA) molecules that target and silence p16 expression, or anti-micro RNA molecules that target and disrupt senescence-associated micro RNA molecules. The use of such inhibitors in ex vivo cell culture methods, treatment of age-related disorders, cell culture media, reperfusion solutions, anti-ageing compositions, anti-wrinkle compositions and wound healing promoting compositions are also provided.
CN101422439A Etoposide freeze-dry powder preparation for injection and preparation method thereof The invention relates to the technical field of medicament and discloses an etoposide freeze-dried powder preparation used for injection, which is convenient to be used in clinic, is high in bioavailability, is low in cost and can cure solid tumors. The medicament can quickly achieve effective curing concentration in a body when being directly injected through vein or muscle; moreover, the first-pass effect of the medicament to a liver is reduced, the bioavailability of the medicament in the body is improved, and the freeze-dried powder preparation used for injection is more convenient to be transported and can be stored for a longer time. The etoposide freeze-dried powder preparation used for injection contains the etoposide or the pharmaceutically acceptable salt thereof and pharmaceutically acceptable accessories used as active components; wherein, the weight percentage of the etoposide or the pharmaceutically acceptable salt thereof can be 1 to 80 percent, preferably be 30 to 70 percent and more preferably be 40 to 60 percent; the content range thereof in the preparation is generally 1 to 1000mg and preferably be 10 to 500mg.
WO2014024136A1 A method of managing diabetic foot ulcers, pressure ulcers, venous leg ulcers and associated complication The present disclosure is related to a method of managing diabetic foot ulcers (DFUs), pressure ulcers, venous leg ulcers and associated complications such as bacterial infection, gangrene, tissue necrosis, amputation, proximal limb loss and septicaemia. This method of managing is by administration of pharmaceutical composition comprising pentameric type A procyanidin, trimeric procyanidin and tetrameric procyanidin, optionally along with pharmaceutically acceptable excipient.
WO2010087244A1 Cyclic amino alcohol compound A novel low-molecular compound having an immunosuppressive action. The compound is a compound having general formula (I) or a pharmacologically acceptable salt thereof. [In the formula, the substituents are defined as shown below: R1 and R2 each represents a hydrogen atom or the like.; R3 represents a hydrogen atom or the like.; Y represents an ethylene group or the like; Z represents a single bond or the like; R5 represents a hydrogen atom or the like; and R6 and R7 each represents a hydrogen atom or the like.]
CN103159646A Hydroxamic acid compound, and preparation method and application thereof The invention relates to the application areas of organic chemistry, pharmaceutical chemistry and medicine, and particularly discloses hydroxamic acid. The hydroxamic acid compound has a structure shown in Formula I, wherein R is selected from a substituted benzene ring, a heterocyclic ring, a substituted heterocyclic ring, a benzoheterocyclic ring or a substituted benzoheterocyclic ring, wherein the substitution refers to that 1-n hydrogen atoms on the benzene ring, heterocyclic ring or benzoheterocyclic ring are substituted by the following groups: halogen, amino, hydroxy, nitro, cyano, alkoxy, aminoalkyl, alkylamino, sulfoalkyl, perfluoroalkyl, perfluoroalkoxy, amido or alkoxycarbonyl. According to the invention, the hydroxamic acid compound achieves the purpose of treating neoplastic diseases by regulating histone deacetylase; the hydroxamic acid compound has anti-proliferation effect on tumor cells, influences cell cycle arrest and induces cell apoptosis; and above all, the anti-proliferation effect on lung cancer cell strains is obviously improved in comparison with the effect of a positive control drug SAHA (suberoylanilide hydroxamic acid).
US20120245561 Intraventricular drug delivery system for improving outcome after a brain injury affecting cerebral blood flow The described invention provides a flowable sustained release microparticulate composition, a kit for treating at least one cerebral artery in a subarachnoid space at risk of interruption due to a brain injury, a method of preparing the composition, and a method for treating an interruption of a cerebral artery in a subarachnoid space at risk of interruption caused by brain injury in a mammal, which reduces signs or symptoms of at least one delayed complication associated with brain injury.
CN103638000A Dispersion preparation containing dabigatran etexilate The invention relates to a dispersion preparation containing dabigatran etexilate. The dispersion preparation mainly comprises a dispersible tablet containing an active substance dabigatran etexilate, and a dispersed particle capsule. The preparation has the characteristics that the preparation can be disintegrated into fine particles in water within three minutes and a uniform suspension is formed. The particles can be evenly distributed and can pass through a 2# sieve (24 meshes). The dissolution rate and the absorption rate of the medicines can be significantly increased after the medicines with poor water solubility are prepared into the dispersion preparation, and the bioavailability is also improved. Meanwhile, the dispersion preparation has the advantages of being convenient to swallow, simple in production technology, high in reproducibility, high in medicine loading rate, easy to divide the dose and the like, and does not change the pH of gastric juice of a sufferer.
US20080274202 Compositions and Method for Brain Specific Targeted Delivery of Therapeutic Agents Disclosed are methods and compositions for delivering a therapeutic agent to target organs or tissues, such as brain. The methods and compositions use bone marrow stem cells, monocytes, macrophages or microglial cells to deliver the therapeutic agent associated with nanoparticles to the target organ or tissue.
WO2006095150A1 Combination of a silicon containing component and a hormone The invention relates to the use of a silicon-containing material to reduce the amount of hormone required in a method of hormone treatment to achieve a desired response, particularly in hormone replacement therapy (HRT) and especially in the maintenance of post-menopausal bone health and the management or treatment of osteoporosis, and to pharmaceutical compositions for use in such a method.
US7371752 such as 5-(4-Fluorophenyl)-7-[(2-pyridyl)-methyloxy]-thieno[3,2-b]pyridine, used as prodrugs or antagonists for GABA receptors, in diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and epileptic disorders, as cognition activators and as antidotes to benzodiazepines Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
US20080214619 Business method to treat and/or prevent a gastric acid disorder with a proton pump inhibitor (PPI) and a cholinergic agonist to induce rapid onset of PPI action with or without food Pharmaceutical proton pump inhibitor (PPI) medications and methods are disclosed for preventing and/or treating gastrointestinal disorders characterized by abnormalities in gastric acid secretion at anytime of the day or night without the need for food effect or to be taken with food. The medications comprise a PPI and a cholinergic agonist for inducing rapid onset of PPI action, for increasing the duration of PPI efficacy and for optimizing clinical PPI effectiveness that may be administered at any time of the day or night without food or on an empty stomach, and possibly on an as-needed or on demand basis. In carrying out the methods, a PPI and cholinergic agonist may be administered together as a single unitary dose in the form of a liquid or solid, or administered together, but separately as either liquids or solids or a combination thereof. Preferably, an oral solid dosage form of the present invention allows for release of a proton pump inhibitor at a pH of about 5 or higher, e.g., pH about 5.5, 6, 6.5 or 7, followed by release of a cholinergic agonist within between about 10 minutes and about 60 minutes, preferably within about 15 minutes and about 30 minutes, after release of the proton pump inhibitor from the dosage form, so that it can be administered at any time of the day or night independent of food or food effect. It is believed that the methods and compositions of the present invention will increase the duration of PPI efficacy by between at least about 5 fold and about 10 fold or even about 20 fold, as compared to the duration of PPI efficacy derived from current PPI dosage forms administered alone and without food or a food effect. Kits comprising a PPI, a cholinergic agonist and optionally an antacid are disclosed, such as kits containing each drug in conventional and commercially available dry or liquid dosage forms for simultaneous or concomitant administration or in dry dosage forms to provide for the easy preparation of a liquid composition from the dry dosage forms. These new medications and methods will simplify the traditional continuous PPI regimen and improve patient compliance.
US20090169591 Medical articles for the treatment of tumors In accordance with one aspect of the invention, implantable and insertable medical articles are provided which are useful for the local treatment of tumors. These medical articles comprise one or more active agents that influence the local tumor environment in vivo, for example, decreasing the level of nutrients in the local tumor environment, inhibiting the utilization of nutrients in the local tumor environment, decreasing the amount of molecular oxygen and/or reactive oxygen species in the local tumor environment, or increasing the amount of molecular oxygen and/or reactive oxygen species in the local tumor environment. Other aspects of the invention pertain to methods of treatment that employ such medical articles. Still other aspects of the invention pertain to methods of making such medical articles.
US20110117172 Cross-linked polymer matrix, in particular for administering active substances The subject is cross-linked polymer matrices, which are used as active substance supports and can be applied locally or parenterally in human or animal bodies. The cross-linked polymer matrices are in particular self-dissolving cross-linked polymer matrices.
CN102657675A Radiation-resisting medicament and preparation method thereof A radiation-resisting medicament and a preparation method thereof relate to a health care product with a radiation-resisting function and a preparation method thereof. In order to solve the problem that the existing radiation-resisting product contains various plant extracts, is unsatisfactory in radiation-resisting effect and complicated in production process due to the fact that various components are contained The radiation-resisting medicament is prepared by main raw materials of blueberry anthocyanin, indigo fruit anthocyanin and auricularian extractives. The preparation method includes: choosing materials, weighing, extracting effective active components and mixing the extractives. The radiation-resisting medicament and the preparation method of...are simple in production process, have the advantages of strengthening immunity, resisting radiation and being convenient to take and fast and complete in absorbing due to the electuary and capsule type proved by cell experiments, and are suitable for all crowd and wide in market prospect.
US20080064749 Lipoxin Analogs as Novel Inhibitors of Angiogenesis The present invention is directed to methods for the prevention or inhibition of angiogenesis. The method is accomplished by the administration of an effective amount of 15-epi-16-(para-fluoro)-phenoxy-lipoxin A4, LXA4, 15-epi-LXA4 or 15-R/S-methyl, LXA4 and pharmaceutically acceptable salts, esters, amides, carboxylic acids, or prodrugs thereof, to a subject in need thereof. As a consequence of the action of the therapeutic agent, angiogenesis is prevented or inhibited in the subject.
US20090257997 Stable Aqueous Compositions Comprising Bioactive Creatine Species Compositions containing one or more bioactive forms of creatine which are aqueous compositions in which the one or more bioactive forms of creatine do not appreciably degrade into creatinine. Also are methods for providing various beneficial effects which comprise administering aqueous compositions comprising at least one creating O-phosphate species to a mammalian subject, either chronically or acutely.
CN102579418A Application of dencichine in preparation of medicament for treating neurodegenerative diseases The invention relates to application of a dencichine medicament, in particular to the application of a small dose of dencichine in preparation of a medicament for treating chronic neurologic diseases. A cytological method is used by researchers of the experiment, so that the condition that a small dose of dencichine can achieve a protection effect on neurogenic cell damages caused by a chronic anoxic effect is proved and a protection effect of a small dose of dencichine on the chronic neurologic diseases is prompted by a cellular morphology observation method, a cellular staining method and other methods by establishing a cellular chronic anoxic model and the like.
US7388020 Compounds for chronic obstructive pulminary disorders for breathingand respiratory system diorders The invention provides compounds of general formula (I) wherein A, X, m, R1, N, R2, Z1, Z2, Q, R3, R4, R5, R6, R7, R8, t and R16 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy
WO2010054260A1 Imidazo[5,1-c][1,2,4]benzotriazine derivatives as inhibitors of phosphodiesterases The invention relates to imidazo[5,1-c][1,2,4]benzotriazine derivatives of formula (I): which are inhibitors of phosphodiesterase 2 or 10 useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.
WO2012135133A1 Lipoxygenase inhibitors The disclosure provides bisindole suitable for inhibiting lipoxygenases or Αβ- formation, and treating associated diseases, such as Alzheimer's disease. The bisindoles are indolo[2,3-b]carbazole derivatives, and may be administered to a patient as part of a pharmaceutical formulation.
EP1581212A2 Superoxide dismutase mimics for the treatment of ocular disorders and diseases The use of SOD mimics, particularly Mn(III) porphyrin complexes, for the treatment of AMD, DR, and retinal edema is disclosed.
US20080234335 2-Cyclohexenyl-1-carboxylic acid derivatives, e.g., 6-[2-(5-chloro-2-{[(4-fluorophenyl)methyl]oxy}phenyl)-1-cyclohexen-1-yl]-2-pyridinecarboxylic acid; treatment of conditions mediated by the action of PGE2 at EP1 receptors such as inflammatory pain, neuropathic pain or visceral pain Compounds of formula (I) wherein A, B, Z, R1, R2a, R2b, R8, R9 and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
US20120208815 Pim kinase inhibitors and methods of their use New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
WO2009143404A1 Piperazine metabotropic glutamate receptor 5 (mglur5) negative allosteric modulators for anxiety/depression The present teachings relate to piperazine metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators having Formula (I); wherein the constituent variables are as defined herein. The present teachings further relate to methods for the preparation of the compounds, and to methods for using the compounds for treatment of diseases and disorders including schizophrenia, paranoia, depression, manic-depressive illness and anxiety.
CN103724342A New antifungal drug compound as well as composition thereof and use The invention relates to a new broad-spectrum antifungal drug compound, a broad-spectrum antifungal drug composition, application of the compound or the composition for preparing a broad-spectrum antifungal drug and application of the compound or the composition for preparing a drug used for treating severe invasive infections caused by invasive aspergillosis and/or fluconazole resistant candida (including candida krusei) and/or serious infections caused by scedosporium spp and fusarium. The new broad-spectrum antifungal drug compound and the broad-spectrum antifungal drug composition have wide and strong antifungal activity, and pharmacodynamic property and the safety are good.
US20120114748 Tanaproget Compositions Containing Ethinyl Estradiol Compositions containing micronized tanaproget, or a pharmaceutically acceptable salt thereof, and ethinyl estradiol and methods of preparing the same are provided. Also provided are kits containing the compositions, methods of contraception and hormone replacement therapy including administering a composition containing micronized tanaproget and ethinyl estradiol.
US20060166992 Heterocyclically substituted imidazotriazines The invention relates to new heterocyclically substituted imidazotriazines, processes for their preparation and their use for the production of medicaments for the treatment and/or prophylaxis of cancer and neurodegenerative disorders, in particular of Parkinson's disease and of schizophrenia.
CN101434631A Estra nitrate ester medicament for inhibiting angiogenesis The invention discloses a compound 1 or salts or ester thereof with a general formula as follows: T-(B-O-NO2)t1, wherein, t1 refers to 1 or 2; T-H refers to a steroidal compound; T refers to steroidal residue obtained from the T-H compound, H of which is removed; oxygen atoms on T are connected with H to form hydroxyl groups, namely, T is connected with H in the form of O-H.
US20100189807 Use of an ozone / oxygen mixture as a primary anticancer therapy via intraperitoneal insufflation Head and neck squamous cell carcinomas (HNSCC) represent a group of metastasizing tumors with a high mortality rate in man and animals. Since the biomolecule ozone was found to inhibit growth of various carcinoma cells in vitro we here applied the highly aggressive and lethal VX2 carcinoma HNSCC tumor model of the New Zealand White rabbit to test whether ozone exerts anti-tumorous effects in vivo. Therapeutic insufflation of medical ozone/oxygen (O3/O2) gas mixture into the peritoneum (O3/O2-pneumoperitoneum) at an advanced stage of tumor disease led to a survival rate of 7/14 rabbits. Six of the seven surviving rabbits presented full tumor regression and the absence of local or distant lung metastases. Insufflation of pure oxygen (O2) resulted in a survival rate of 3/13 animals accompanied by full tumor remission in two of the three surviving animals. Of the fourteen sham-treated animals only one had spontaneous tumor remission and survived. No adverse effects or changes in standard blood parameters were observed after repeated intraperitoneal insufflations of the O3/O2 or O2 gas. Animals with O3/O2-induced tumor eradication developed tolerance against re-implantation of the VX2 tumor. This could be reversed by immune suppression with a combination of dexamethasone and cyclosporin A suggesting an anti-tumorous effect of O3/O2-mediated activation of the body's own immunosurveillance. Although the exact mechanisms of action are still unclear the present data point to O3/O2-pneumoperitoneum as a promising new strategy in anticancer therapy.
CN101940599A Liquid for preventing and treating human diseases The invention relates to a liquid for preventing and treating human diseases, which can efficiently solve the problem on finally completing the in vivo synthesis of endogenous morphine peptide so as to achieve the purposes of disease prevention and treatment. The technical scheme of the invention for solving the problem comprises the following steps of: adding 1000 ml of purified water to 155-185 g of eggs hatched for 7 days, pounding the eggs by using a pounding machine under 18000-22000 RPM, and standing for reaction for 31-35 h at the temperature of 50-52 DEG C to obtain the liquid for preventing and treating human diseases. The invention has the advantages of simple method, low cost, easy preparation, convenient taking and good prevention and treatment effect, and the liquid is a great creation for preventing and treating the human diseases.
US20100113409 Hydrochloride salt of 5-[3-(3-hydroxyphenoxy) azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide This invention relates to the hydrochloride salt of 5-[3-{3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenyl-hexanamide or derived form thereof and its use as a medicament.
WO2005035574A1 IgM HIGH CONCENTRATION STABILIZED SOLUTION The use of a compound containing a multi-valent cationic ion, such as magnesium chloride or arginine hydrochloride, as an additive, has allowed the inhibition of the association of IgM in a solution, resulting in the preparation of an IgM solution which has a high concentration and also is stable.
CN101039671A Non-peptide bradykinin antagonists and pharmaceutical compositions therefrom Non-peptide compounds having activity as selective antagonists of bradykinin (BK) B2 receptor. The compounds are chemically characterized by the presence of an amino acid alpha substituted with a cyclic group and by a tetraalkylammonium group.
CN103110613A Application of saturated amine compound in preparation of anti-radiation damage medicament The invention discloses application of a saturated amine compound in preparation of an anti-radiation damage medicament. Experiments prove that the saturated amine compound can improve the contents of white blood cells (WBC), red blood cells (RBC) and platelets (PLT) in peripheral blood of animals damaged by radiation, promotes proliferation of bone marrow hematopoietic stem/progenitor cells and recovery of a hematopoietic system, and has good repairing effect on intestines, livers and lung tissues of mice damaged by the radiation, and can obviously improve the survival rate of animals damaged by the radiation. The application of the unsaturated amine compound in the preparation of the anti-radiation damage medicament provides a new thought for the research and development of the anti-radiation medicament, and is wide in application prospect and immeasurable in significance.
US20050245512 Method and composition for rejuvinating cells, tissues organs, hair and nails In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated coupling of proteins, lipids, nucleic acids, and other biomaterials, and any combination thereof. In another embodiment, the compositions and associated methods have utility in vivo to reduce the deleterious effects of sugar-mediated coupling processes in an organism, when the organism is exposed to the compound or composition internally, by ingestion, transdermal application, or other means. In yet another embodiment, the compositions and associated methods are useful for the ex-vivo treatment of organs, cells and tissues and external treatment of hair, nails and skin to rejuvenate them by changing deformability and increase the tissue diffusion coefficient. In a further embodiment, the present invention relates to novel compounds and pharmaceutical compositions.
CA2369095C Anticonvulsant derivatives useful in treating chronic neurodegenerative disorders Use of anticonvulsant derivatives of formula (I) for treating chronic neurodegenerative conditions, wherein X is CH2 or oxygen; R1 is hydrogen or C1-C4 alkyl; and R2, R3, R4 and R5 are independently hydrogen or alkyl and, when X is CH2, R4 and R5 may be alkene groups joined to form a benzene ring and, when X is oxygen, R2 and R3 and/or R4 and R5 together may be a methylenedioxy group of formula (II), wherein R6 and R7 are the same or different and are hydrogen, or alkyl and are joined to form a cyclopentyl or cyclohexyl ring.
US8263600 Antifungal composition with enhanced bioavailability A liquid suspension comprising an antifungally effective amount of the micronized compound represented by the chemical structural formula I: at least one thickening agent, a non-ionic surfactant, and a pharmaceutically acceptable liquid carrier is disclosed.
CN102973559A Novel method of applying oxymatrine to treating eczematous dermatitis The invention provides a novel method of applying oxymatrine to treating eczematous dermatitis, belonging to the field of medicines. The method is characterized by 1. adopting intravenous drip of oxymatrine to treat eczematous dermatitis, 2. adopting intravenous drip of oxymatrine to treat eczematous dermatitis in combination with oral administration of antihistamines, 3. adopting oral administration of oxymatrine tablets or capsules to treat eczematous dermatitis and 4. applying oxymatrine ointments to the wounded parts to externally treat eczematous dermatitis. Compared with the existing medicines and methods for treating eczematous dermatitis, the novel method has the effects that unexpected curative effects can be obtained and the cure rate is above 75%. The new method is an innovative idea of holistic treatment for treating eczematous dermatitis and has great medical significance.
CA2229479C Method of promoting angiogenesis Relaxin is useful for promoting angiogenesis and the treatment of infections or ischemic wounds where the injury results from lack of oxygen due to poor circulation.
US20070293554 Non-peptide inhibition of T-lymphocyte activation and therapies related thereto Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium-activated K+ channel (IKCa1) in lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-, cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca++ activated K+ channel (IKCa1) prevents the pre-Ca++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.
US20110046083 Activators of pyruvate kinase m2 and methods of treating disease The invention described herein features methods, compositions, and kits for the use of activators of PKM2 for the treatment, prevention, or amelioration of diseases related to PKM2 function, including, e.g., cancer, diabetes, atherosclerosis, restenosis, obesity, autoimmune disorders, and proliferative disorders.
CN1875981A Injection emulsion containing breviscapinum and preparation method thereof The invention relates to an emulsion injection containing Breviscapine and its preparing process, which is prepared from the following raw materials (by weight portion): Breviscapine 0.01-0.04%, oil for injection 5-30%, emulsifying agent 1-5%, isotonic agent 2-10%, stabilizer 0.1-8% and balancing water for injection. The preparation process comprises the steps of proportioning, making oily phase mixture, making initial milk, emulsifying and sterilizing.
CN101040895A Medicine for improving immunity The invention discloses a drug for improving immunity, formed by jade shield and decaris at 9:0.10-0.20. Compared with single drug of jade shield and decaris, the inventive drug can improve effect and reduce the side effect of decaris, in particular for processing group immunity in on serious epidemic disease.
US20110274698 Immunomodulation Of Inflammatory Conditions Utilizing Follistatin-Like Protein-1 And Agents That Bind Thereto Follistatin-like protein (FSTL-1) is a secreted glycoprotein of unknown function, first isolated from mouse osteoblastic cells as a transforming growth factor-β1-inducible gene. The inventors have discovered that FSTL-1 is a proinflammatory mediator. As such, the invention provides for composition and methods of using agents that bind to FSTL-1 to modulate various types of inflammation (e.g., autoimmune diseases). Inhibitors and antagonists of FSTL-1, particularly antibodies or antibody fragments, may be used to treat conditions related to inflammation, such as arthritis. In addition, the inventors have discovered that FSTL-1 has a role in the Th17 pathway. Accordingly, the invention provides for compositions and methods of using agents which bind to FSTL-1 to modulate the generation of Th17 cells. Such agents are useful for delaying development of and treating diseases associated with undesired production of Th17 cells, such as autoimmune diseases. Furthermore, since FSTL-1 is a proinflammatory mediator with a role in cancer, the invention provides for compositions and methods of using a pharmaceutical composition of FSTL-1 to delay development of or treat cancer.
CN102106809B Solid preparation of clopidogrel and preparation method thereof The invention belongs to the field of medicinal preparations, and relates to a solid preparation and a preparation method thereof, in particular to a solid preparation of clopidogrel or pharmaceutically acceptable salt of the clopidogrel as well as a preparation method thereof. The solid preparation is mainly prepared by mixing the clopidogrel or the pharmaceutically acceptable salt thereof with dimeticone and then processing the obtained mixture according to a conventional solid preparation processing method. By adopting the dimeticone, the invention has the advantages of preventing a dextroisomer of the clopidogrel from converting into a levoisomer, preventing the clopidogrel from being degraded into clopidogrel acid, being applicable to the formula and process for large-scale production of the preparation, solving the problem of drug degradation, improving drug stability, solving sticking and picking phenomena during the tabletting process, and improving product quality.
CN101264308A Health care drinking liquid for preventing and controlling influenza The invention discloses a health Yinye for preventing and controlling influenza, comprising the following raw medicines according to the weight account: liquorice 10 to 20 parts, largehead atractylodes rhizome 10 to 20 parts, schisandra chinensic 10 to 20 parts, catnip 10 to 20 parts, plaster 10 to 20 parts, jujube 5 to 10 parts, vane ladybell Root 20 to 40 parts, and ginger 5 to 10 parts. The health Yinye has the advantages of improving body immune function, reinforcing body antiviral ability, preventing and controlling influenza rapidly and effectively, and preventing infection of influenza virus for long time without any poison and side effects, having effectivity, safety and ability to be used for long time.
CA2620363A1 Naphthalene-disulfonamides useful for the treatment of inflammation There is provided compounds of formula (I), wherein R1, R2, X2, X4 and X5to X8 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.
WO2009117157A1 Aurora kinase modulators and method of use The present invention relates to chemical compounds having a general formula (I) wherein A1-5 and 7-8, D', L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
WO2014081392A8 Composition and method for respiratory delivery of dye for visualisation of eye The present invention relates to a composition and method for respiratory delivery of a dye for visualising the eye of a subject. Respiratory delivery for a dye for visualisation is suitable for visualising the eye for the detection, diagnosis and/or monitoring of eye conditions in a wide population of subjects, especially where intravenous dye delivery is contraindicated or undesirable (e.g.in the elderly, children, diabetic subjects or where suitable veins for intravenous injection are difficult to find).
EP1085855A4 Enhanced intra vaginal devices Intra vaginal devices having an improved in vivo performance insofar as release characteristics are concerned. The devices rely on a polymer matrix impregnated not only with the active ingredient (e.g.: progesterone) to be released but also a suitable cyclodextrin. Suitable polymers include poly (ε-caprolactone) and starch-like polysaccharides.
WO2008128166A1 Deuterated derivatives of 4-(6-fluoro-1, 2-benzisoxazol-3-yl) piperidine compounds This invention relates to novel 1, 2-benzisoxazol-3-yl compounds of formula (I), their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an antagonist of both dopamine and serotonin receptors. (I), wherein:at least one R group (i.e., R1a, R1b, R2, R3a, and R3b) comprises a deuterium atom.
WO2014037381A1 Method for treating pruritus Benzomorphan compounds are found to be useful for treating, ameliorating or preventing pruritus, and in particular pruritus associated with (including induced by) the administration of opioids. Antipruritic activity is believed to be mediated through the dual action of the compounds as mu opioid receptor antagonists and kappa opioid receptor agonists. Pharmaceutical compositions contain therapeutically effective amounts of these useful compounds, optionally in combination with second therapeutic agents, such as opioid or non-opioid analgesics or other compounds.
CN1872071A Medication for enhancing body immunity, and fighting against senium, and preparation method A medicine for improving immunity and delaying sanility is disclosed. Its advantages are high natural level and safety and low toxic by-effect.
CN101879145A Anti-HIV drug zidovudine for injection and preparation process thereof The invention discloses an anti-HIV drug zidovudine for injection and a preparation process thereof, and the zidovudine for injection is prepared by firstly using water for injection at the temperature of 55-60 DEG C for preparation and then carrying out filling, freeze-drying and other steps. The product prepared by the process has stable quality, low investment in excipients, capability of retaining the activity of main ingredients to the maximum extent, loose texture, complete framework, good product form, low bottle breakage rate of below 1% and high product yield of above 98%.
EP1117667B1 BENZOTHIENO[3,2-c]PYRIDINES AS ALPHA2 ANTAGONISTS The present invention concerns the compounds of formula (I), the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C¿1-6? alkyl, nitro, hydroxy or C1-4 alkyloxy; Alk is C1-6 alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central α2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.
WO2012128417A1 Water-soluble cationic-drug delivery system having a sustained-release mechanism The present invention relates to a water-soluble cationic-drug delivery system having sustained release behavior in which a drug having a positive charge and a compound containing polyanions form an ion complex. According to the water-soluble cationic-drug delivery system, not only may a drug be effectively locally delivered to a diseased area through the sustained-release mechanism, but the frequency of medication may be significantly reduced. Thus, the hassle of frequent visits to the hospital to treat lesions and the associated medical costs may be significantly reduced.
WO2004105775A8 Pharmaceutical composition comprising glucan derived from microalgae The present invention describes a pharmaceutical composition having immunostimulatinf, prophylactic and/or growth enhancing effects by enhancing the overall resistance against diseases caused by pathogenic and opportunistic pathogenic microorganisms, comprising microalgae containing glucan or glucan derived from microalgae.
US20090074882 Insulin compositions and method of making a composition The invention is related to insulin compositions with a high content of zinc atoms per six molecules of acylated insulin. The insulin is an acylated insulin and may be mixed with a further insulin analogue such as the rapid acting insulin Asp B28 human insulin.
US20100015201 Implant with coating The present invention concerns an implant with a molecularly imprinted polymer coating, a process for its synthesis, a molecularly imprinted polymer, as well as a process for its synthesis and its use as well as a process for the treatment or prophylaxis of certain disease conditions by implantation of an implant in accordance with the invention according to the respective independent claims.
CN101590096A Medicinal composition for reducing blood fat The invention provides a medicinal composition for reducing blood fat. The composition comprises fiveleaf gynostemma herb, vitamin B complex, vitamin E and trace elements zinc, selenium, chromium, copper, molybdenum, iodine and manganese. The medicinal composition is mainly suitable for tall blood fat crowd, is effective in the aspect of reducing the blood fat, and can be applied for long term or according to treatment courses.
DE102005037096A1 Medicament, useful to treat or prevent e.g. viral infections, comprises a combination of iron-oxide, ferric oxide hydrate, magnetite and/or hematite and a lanthanide compound Medicament (A) comprises a combination of iron(III)-oxide, ferric oxide hydrate, iron(II, III)-oxide, magnetite and/or hematite and a lanthanide compound. Independent claims are included for: (1) a medicament containing one or more compounds; (2) an infusion solution; (3) an injection solution for intravenous injection; (4) use of an active agent or the active agent mixture in gene technological; and (5) the manufacture of the active agent through cultivation, separation or isolation. - ACTIVITY : Virucide; Anti-HIV; Antiinflammatory; Hepatotropic. - MECHANISM OF ACTION : None given.
US7807185 applying to skin or mucous membrane of a mammal a composition comprising an extracellular product of a Pseudomonas lindbergii strain, an extracellular product of a Bacillus coagulans strain, and an anti-fungal agent selected from Amphotericin B, Carbol-Fuchsin, Ciclopirox, for example The present invention discloses compositions derived from an isolated Bacillus species, spores, or an extracellular product of Bacillus coagulans comprising a supernatant or filtrate of a culture of said Bacillus coagulans strain, suitable for topical application to the skin or mucosal membranes of a mammal, which are utilized to inhibit the growth of bacterium, yeast, fungi, virus, and combinations thereof. The present invention also discloses methods of treatment and therapeutic systems for inhibiting the growth of bacterium, yeast, fungi, virus, and combinations thereof, by topical application of therapeutic compositions which are comprised, in part, of isolated Bacillus species, spores, or an extracellular product of Bacillus coagulans comprising a supernatant or filtrate of a culture of said Bacillus coagulans strain. In addition, the present invention also discloses compositions, methods of treatment, and therapeutic systems for inhibiting the growth of bacterium, yeast, fungi, virus, and combinations thereof, comprising an extracellular product of Pseudomonas lindbergii comprising a supernatant or filtrate of a culture of said Pseudomonas lindbergii strain.
WO2014143643A1 Acyclic nucleoside phosphonate diesters The present disclosure relates, inter alia, to compositions and methods for treating viral diseases and cancer. There are disclosed lipophilic antiviral and anticancer acyclic nucleoside phosphonate diesters, preparation thereof, and methods of using the compounds to treat viral diseases and cancer.
CN1679567A Granules of clarityne and their production A particle of loratadine is prepared proportionally from loratadine, citric acid, and the additive chosen from edible essence, sweetening agent and edible pigment.
US7727712 Having an immunostimulatory sequence comprising the sequence 5'-C, G-3', wherein an HBV antigen is not administered in conjunction with administration of said nucleotide; for treatment of subject with hepatitis B virus Methods are provided for the treatment of hepatitis B virus (HBV) and hepatitis C virus (HCV) infections. A polynucleotide comprising an immunostimulatory sequence is administered to a individual who has been exposed to or infected by HBV and/or HCV. The polynucleotide is not administered with a HCV or HBV antigen. Administration of the polynucleotide results in amelioration of symptoms of HBV and/or HCV infection.
US20060276415 5-Beta-sapogenin and pseudosapogenin derivatives and their use in the treatment of dementia The invention discloses the use of sapogenin derivatives in the treatment of cognitive disfunction and similar conditions. Methods of treatment and pharmaceutical compositions are also disclosed
CN102952129A Tetrahydropyridodihydropyrimidinone derivative, its preparation method and application Relating to the field of medical chemistry, the invention discloses a tetrahydropyridodihydropyrimidinone derivative, the structure of which is shown as formula (I). Specifically, R1 is hydrogen, an alkyl group, an alkoxyl group or halogen, R2 is a substituent group of position 2, 3 or 4 of a benzene ring, and can be one of an alkyl group, an alkoxyl group, halogen, a nitro group, a carboxy group, a cyano group, or an ester group. The tetrahydropyridodihydropyrimidinone derivative has good inhibitory activity on proliferation of leukemia K562 cells, proliferation of ovarian cancer HO-8910 cells and proliferation of SMMC-7721 hepatoma cells, and can be used for preparing medicines treating leukemia, ovarian cancer and hepatoma.
US20100298411 Lipid-modified double-stranded rna having potent rna interference effect An object of the present invention is to provide a novel double-stranded RNA that has high nuclease resistance and high cellular uptake efficiency, and that is capable of producing an excellent RNA interference effect. The present invention provides a lipid-modified double-stranded RNA comprising a sense strand having a nucleotide sequence complementary to a target sequence, and an antisense strand having a nucleotide sequence complementary to the sense strand, the double-stranded RNA being capable of inhibiting the expression of the target gene, the sense strand having a lipid linked to at least one of the first to sixth nucleotides from the 5′ end side directly or via a linker.
US20100330130 Substantially pure imatinib or a pharmaceutically acceptable salt thereof Provided herein are impurities of imatinib, N-(2-Methyl-5-methylamino-phenyl)-N-(4-pyridin-3-yl-pyrimidin-2-yl)-formamide (formamide impurity) and 4-[4-(Imidazole-1-carbonyl)-piperazin-1-ylmethyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide (carbonylimidazole impurity), and processes for the preparation and isolation thereof. Provided further herein is a highly pure imatinib or a pharmaceutically acceptable salt thereof substantially free of formamide and carbonylimidazole impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure imatinib or a pharmaceutically acceptable salt thereof substantially free of impurities. Disclosed also herein is a process for preparing substantially pure α-form of imatinib mesylate.
EP2468743A1 Nitrogen-containing bicyclic compounds useful as antibacterial agents A nitrogen-containing heterocyclic compound represented by the general formula: wherein the dashed line represents a single bond or a double bond; R1, R2, R3, R4 and R5 independently represent a hydrogen atom, halogen atom, a lower alkyl, aryl, lower alkoxy or monocyclic heterocyclic group which may be substituted or the like; R6 represents a lower alkyl, aryl, monocyclic heterocyclic, bicyclic heterocyclic or tricyclic heterocyclic group which may be substituted; X1 represents a lower alkylene group or the like; X2 represents a lower alkylene, lower alkenylene or lower alkynylene group which may be substituted; X3 represents an oxygen atom, sulfur atom, a sulfinyl group, sulfonyl group or the like; Y1 represents a bivalent cyclic group, containing a nitrogen, which may be substituted or the like; and Z1 represents a nitrogen atom, a carbon atom which may be substituted or the like, or a salt thereof. The compound or salt has a potent antibacterial activity and a high safety, and is therefore useful as an excellent antibacterial agent.
CN101288673A Minocycline hydrochloride microballoons and preparation method and application in pharmacy thereof The invention relates to a minocycline hydrochloride microsphere, a preparation method thereof and the application thereof in medicine preparation; the invention is technically characterized in that the components comprise minocycline hydrochloride drug, biodegradable polymer material, emulsifier and chemical cross-linking reagent; the weight percentage of the components is 10 percent to 20 percent (W/W) of minocycline hydrochloride, 15 percent to 40 percent (W/W) of biodegradable polymer material; the ratio between biodegradable polymer material and chemical cross-linking reagent is 1g : 5mL to 1g : 20mL; the volume ratio between aqueous phase and fat phase is 1 : 10 to 1 : 20 (V/V). The minocycline hydrochloride microsphere and the related preparation thereof (such as jellies) prepared by the invention not only has the remarkable advantages of avoiding the toxic and side effects resulted from systemic antibiotics use, being able to reach the depth of periodontal pocket, sustained-release of the medicine at the bottom (one dose can result in continuous release for 7 days), etc., but also greatly reduces the marketing price owing to the cost reduction resulted from totally using home-made excipients, which is beneficial for reducing the patient burden.
US7678810 activin receptor-like kinase 5 (ALK5) (which is a TGF- beta type I receptor) inhibitor ; glomerulonephritis, diabetic nephropathy, hepatic fibrosis, liver cirrhosis, pulmonary fibrosis, or alopeciarosis; hair growth stimulant A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.
US20080090812 Pyrrolobenzodiazepine Therapeutic Agents Useful in the Treatment of Leukemias A pyrrolobenzodiazepine dimer compound of Formula (I): or pharmaceutically acceptable salt or solvate thereof is useful as a therapeutic agent for the treatment of leukaemias, especially B-cell leukaemias, that exhibit resistance to other chemotherapeutic drugs, wherein: the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R2 and R3 are independently selected from —H, ═O, ═CH2, —CN, —R, OR, halo, ═CH—R, O—SO2—R, CO2R and COR; R6, R7 and R9 are independently selected from II, R, OII, OR, SII, SR, NII2, NIIR, NRR′, nitro, Me3Sn and halo; where R and R′ are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 is a carbamate-based nitrogen protecting group and R15 is either O—R11, wherein R is an oxygen protecting group, or OH, or R10 and R15 together form a double bond between N10 and C11; R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings, and each X is independently selected from 0, S, or NH; R2′, R3′, R6′, R7′, R9′, R10′ and R15′ are all independently selected from the same lists as previously defined for R2, R3, R6, R7, R9, R10 and R15 respectively.
US20080279948 Treatment of Asthma and Copd Using Triple-Combination Therapy A medicament comprising, separately or together (A) a compound of formula I in free or salt or solvate form, wherein W, Rx, Ry, R1, R2, R3, R4, R5, R6 and R7 have the meanings as indicated in the specification; (B) a glycopyrronium salt; and (C) mometasone furoate; for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.
CA2659184C Ep2 agonists The invention provides EP2 agonists, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for lowering intraocular pressure and thereby treating glaucoma. In one particular embodiment, there is provided a compound of the formula: (see above formula) or a pharmaceutically acceptable salt thereof.
WO2005021009A2 Formulations and methods of treating inflammatory bowel disease Methods and formulations for treating inflammatory bowel disease are disclosed. The methods and formulations include methods and formulations for delivering eff ective concentrations of 4-aminosalicylic acid and/or 5-aminosalicylic acid to o r their salts and prodrugs, such as 4,4'- azo-bis salicylic acid affected areas of the intestine. The methods and formulations comprise modified-release element s, providing for drug delivery to the affected or desired area. Diseases and con ditions treatable with the present invention include Crohn?s disease and ulcerat ive colitis.
CN1644203A Oral preparation of red common stone crop polysaccharide and its making method An oral compound medicine of salidroside in the form of tablet and capsule for improving immunity, decreasing blood sugar and blood fat, relieving fatigue and delaying senility is prepared from rhodiola root through extracting its polyose, salidroside and volatile oil, proportional mixing and shaping.
CN103193743A Compound, preparation method for compound and application of compound in preparation of anti-tumor medicament The invention discloses a compound, a preparation method for the compound and application of the compound in preparation of an anti-tumor medicament. The invention protects the compound shown as formula (I) and the application of the compound shown as formula (I) in preparation of a product for inhibiting tumor cell proliferation. The invention also protects the application of the compound shown as formula (I) in preparation of a product for treating and/or preventing tumors. The invention discloses a new compound, and provides the application of the compound in inhibition of tumor cell proliferation and the preparation method for the compound. The compound has an inhibiting effect on multiple tumor cells, and can be used for developing cell proliferation inhibitors and anti-tumor medicaments.
EP2293793A1 2,5-disubstituted imidazo[4,5-c]pyridines for treating muscular dystrophy Compounds of formula (I): wherein R1, R2, R3, and n are as defined herein, are useful for the treatment or prophylaxis of Duchenne muscular dystrophy, Becker muscular dystrophy, or cachexia.
CN1895267A Composite gel of CMC and collagen synthase inhibitor for preventing adhered Fe crosslinked and its preparation An anti-adhesion compound gel for surgical operation is prepared from Fe ion cross-linked CMC, collagen synthetase depressant and PBS solution. Its preparing process is also disclosed.
US20090149469 Phenyl-[4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl]-amine derivatives as igf-ir inhibitors The present invention relates to a compound of formula I and derivatives thereof. Furthermore, the invention relates to the use of such compounds as medicaments. In addition, the invention relates to the use of such compounds for manufacturing a medicament useful for treating proliferative diseases.
EP0549592B2 Stabilized retinoid-containing skin care compositions Skin care compositions comprising a water-in-oil emulsion base containing retinoids and possessing good physical and chemical stability.
CN102793659A Aspirin suppository and preparation method thereof The invention provides an aspirin suppository suitable for cavitary drug delivery and a preparation method thereof. The suppository is prepared from the following raw materials by weight part: 10-20 of aspirin, 7-12 of sodium carboxymethylcellulose, 14-28 of an oleaginous matrix (such as coconut oil ester, Litsea cubeba oil, palmitate, propylene glycol stearate and the like), 35-95 of a water soluble matrix (such as glycerol, gelatin, polyethylene glycol and the like), and 5-10 of a hardening agent (such as white wax, stearic acid, carnauba wax and the like). The drug provided in the invention can be absorbed directly from an intestinal canal, so that the destruction of a liver first-pass effect during oral administration can be avoided. The drug has the advantages of uniform dispersion, stable dissolution rate, and bioavailability improvement, thus being an effective way of administration.
WO2007139240A1 7-(3,4-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds, process for preparing thereof, and pharmaceutical composition for treating or preventing asthma, chronic obstructive pulmonary disease, arthritis, atopic dermatitis, tumor and degenerative brain diseases comprising the same The present invention relates to 7- (3,4- dialkoxyphenyl) -pyrazolo [1, 5 -a] pyrimidine compounds, pharmaceutically acceptable salts thereof, preparation thereof and pharmaceutical compositions comprising the same as an active ingredient for treating or preventing inflammatory diseases including asthma and chronic obstructive pulmonary disease, arthritis, atopic dermatitis, cancers including leukemia, and degenerative brain diseases such as Alzheimer disease, depression or failure of memory.
US6858593 Composition in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in the crystalline composition is of space group P212121 having unit cell dimensions of about 7. 6+-0.6 Angstrom , 12.7+-0.7 Angstrom , There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in the crystalline composition is of space group P212121 having unit cell dimensions of about 7.6±0.6 Å, 12.7±0.7 Å, and 33±3 Å when determined at 120 K.
CN102657661A Pharmaceutical application of Nestorone in preparing Alzheimer disease The invention provides an application of Nestorone (16-methylene-17 alpha-acetoxy-19-nor-pregna-4-alkene-3,20- diketone, Nes) in preparing neuroprotective medicines for improving and treating Alzheimer disease. The prepared medicine contains medicinal excipient vehicles or carriers which are allowed in the preparation, and the dosage forms comprise liquid preparations, granules, sustained-release preparations, electuary, tablets, or capsules. According to the invention, Nestorone used as the neuroprotective medicines for improving and treating Alzheimer disease and the application thereof are demonstrated on a cellular level. Compared with progesterone, Nestorone has stronger curative effect in improving and treating Alzheimer disease and lower toxic and side effect in nervous system.
WO2013135727A1 Glioma treatment by convection enhanced delivery The present invention provides a chemotherapy agent or a pharmaceutical composition comprising a chemotherapy agent and artificial cerebrospinal fluid, wherein the chemotherapy agent is at a concentration of between 0.01mg/ml and 0.7mg/ml, for use in the treatment of brain cancer, in particular a glioma, via convection enhanced delivery.
EP1494543A1 Dietary methods for canine performance enhancement A method for increasing the hunt performance of a hunting mammal which includes orally administering to the mammal an effective amount of a diet comprising unsaturated fatty acid eicosapentaenoic acid (EPA), unsaturated fatty acid docosahexaenoic acid (DHA), or both unsaturated fatty acids, in a total amount of the diet greater than about 0.20 weight percent. The invention also provides dietary compositions that yield other beneficial results.
US20100221319 Compositions and Methods for Improved Skin Care Compositions and methods for administering collagen to a human subject have been developed. The collagen-containing lipid vesicles of the invention provide a delivery system for human collagen which eliminates problems associated with chemical and physical instability of the collagen as well as immune responses to non-human collagen.
CN103142728A Pure herbal heat-clearing oral liquid and preparation method thereof The invention discloses a strangury-clearing oral liquid of and a preparation method thereof. The strangury-clearing oral liquid comprises the following ingredients, by weight, 30 parts of fringed pink, 30 parts of knotgrass, 30 parts of Aristolochia manshuriensis Kom, 30 parts of plantago seeds (salt stir-fried), 30 parts of talcium, 30 parts of cape jasmine fruit, 30 parts of rhubarb, and 30 parts of licorice (fried). The strangury-clearing oral liquid provided by the invention is a pure herbal pharmaceutical composition oral liquid dosage form, is prepared based on strangury-clearing granules prescription formula in the volume I of Chinese Pharmacopoeia (2010 edition), has the efficacies of clearing heat, purging fire, draining water, and relieving strangury, and can be used for bladder damp-heat, frequent and difficult painful urination, dribbling urination, difficult urination, abdominal distension, and dry mouth and throat. Compared with the strangury-clearing granules on the pharmacopoeia standards and conventional strangury-clearing oral solid preparations such as strangury-clearing tablets and strangury-clearing soluble granules, the strangury-clearing oral liquid has the advantages of small orally taken dose, good taste, convenience for taking, rapid absorption, high bioavailability, stable quality, simple production process, etc.
CN101869655A Quick-acting scarless burn and scald ointment The invention provides quick-acting scarless burn and scald ointment. The ointment comprises the following components in weight proportion: the ratio of rheum officinale: tendril-leaved fritillary bulb: compound sulfamethoxazole: sulfadiazine: gentamicin: borneol: bark oil: Vaseline: cefradine is (15-25):(8-12):(10-20):(0-12):(2-6):(3-8):(5-7):(85-125):(0-1). The drugs are weighed and mixed in specified amount, are grinded and mixed to prepare the ointment. The burn and scald ointment can treat various burn and scald wounds, has short course of treatment, and scars cannot be left after healing.
WO2006090717A1 Quinazoline derivative having tyrosine kinase inhibitory activity A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate of the compound or the salt: (I) wherein Rx represents a group represented by the formula(II): where R1 represents a hydrogen atom, an alkyl group which may be substituted or the like, Z represents -O-, -N(R10)- or the like, R10 represents a hydrogen atom, an alkyl group or the like, R2 represents a hydrogen atom, an alkyl group which may be substituted or the like, R18 represents a hydrogen atom, an alkyl group which may be substituted or the like, R19 represents an alkyl group which may be substituted or the like, W1 represents a non-aromatic nitrogenated heterocyclic group which may be substituted, and R17 represents a hydrogen atom, an alkyl group which may be substituted or the like; R3 and R4 independently represent a hydrogen atom, an alkyl group which may be substituted or the like; X represents -O-, -S-, -N(R12)- or the like; R12 represents a hydrogen atom, an alkyl group or the like; and A represents a phenyl group which may be substituted or the like. The compound can inhibit both EGF receptor tyrosine kinase and HER2 tyrosine kinase.
US20120039844 Composition and use of n-alpha-methylhistamine dihydrochloride for the reduction of oxygen radical formation An improved composition and method for reducing the formation of oxygen radicals in mononuclear phagocytes is disclosed. Also provided is a method of protecting NK cells from oxidative damage inflicted by radicals produced by mononuclear phagocytes by administering a histamine metabolite, N-alpha-methylhistamine dihydrochloride. Use of N-alpha-methylhistamine dihydrochloride for enhancing the NK cell response to IL-2 is likewise detailed.
US20090076122 PARP Modulators and Treatment of Cancer The invention relates to a method of modulating poly(ADP-ribose)polymerase-1 (PARP-1) activity in a mammal comprising administering to a mammal an effective amount of an organic aromatic compound having from 4 to about 35 carbon atoms, wherein said organic aromatic compound is capable of binding the arginine-34 moiety located in Zinc finger-1 of the PARP-1 enzyme and wherein said organic aromatic compound has electron donating capabilities such that it's π-electron system will interact with the positively charged (cationic) guanidinium moiety of the specific arginine-34 residue of the Zinc-1 finger of PARP-1 and does not contain benzamide or lactam substituents. In particular, substituted benzopyrones and substituted indoles and their pharmaceutical compositions containing such compounds that modulate the activity of PARP-1, are described. The invention is also directed to the composition of matter, kits and methods for their therapeutic and/or prophylactic use in treating diseases and disorders described herein, by administering effective amounts of such compounds. Preferably, the compositions and methods provided herein inhibit PARP activity.
CN102048707A Mesalazine enteric-coated tablet and preparation method thereof The invention provides a mesalazine enteric-coated tablet and a preparation method thereof. The mesalazine enteric-coated tablet is characterized in that an oblate mesalazine plain film with the diameter of 1.0-1.3cm is used as a tablet base, and the surface of the oblate mesalazine plain film is sprayed and coated with an enteric-coated film coat layer with the thickness of 0.6-1.2mm. The plain film of the enteric-coated tablet is prepared from accessories, such as mesalazine, lactose, microcrystalline cellulose, sodium carboxymethyl starch, polyvidone K30 and talcum powder, the enteric-coated coat layer is an enteric-coated material Yixinke-EOBS68 ethanol solution of Aileyi cooperation, and the enteric-coated film coat layer with the thickness of 0.6-1.2mm is formed on the surface of the mesalazine plain film. The invention has the advantages of lessened tablet crushing rate, improved yield, high drying speed, lessened tablet influence by heat, improved tablet quality, good dampproof performance, enhanced tablet stability and improved tablet dissolution rate so that the tables is rapid to disintegrate, has high effect and improves the bioavailability and the clinical curative effect.
EP2620151A1 Use of adrenergic beta-3-receptor blockers in cancer treatment An adrenergic beta-3-receptor blocker for use as a medicament for treatment of a cancer disease is disclosed. The adrenergic beta-3-receptor blocker is preferably SR59230A and its derivatives.
CN102731397A Preparation method of compound isocorydione having anticancer activity The invention discloses a preparation method of a compound isocorydione having anticancer activity. Isocorydione as a raw material undergoes an oxidation one-step synthesis reaction in the presence of an oxidant to produce the compound isocorydione having anticancer activity. Through chemical conversion, the problems that the content of isocorydione in a plant is low and a large amount of the compound isocorydione having anticancer activity is prepared by a natural product extraction separation method difficultly are solved. The preparation method is simple and practical.
CN1778802A Crystal form of Peimeiqusai disodium and its preparation A crystal form of folic acid antagonistic N-(4-(2-(2-amino-4,7-methyl-4-oxo-1H-pyrrolo(2,3-d)pyrimidine-5-radical)ethyl)benzoyl)-L-glutamic acid disodium salt and its production are disclosed.
US20120277234 1,2,4-oxadiazole benzoic acids Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.
US20120040914 Enhancing effectiveness of glial cancer therapies A method of enhancing the effectiveness of a chemotherapeutic agent, such as Temozolomide (TMZ), or ionizing radiation against glioblastoma is described in the present invention. The method comprises targeting putative membrane androgen receptor (termed mAR) in glioma cells to enhance the cytotoxic effects of a chemotherapeutic agent or ionizing radiation while simultaneously affording protection to neighboring neurons.
WO2011150682A1 4-hydroxyquinoline-3-amide derivatives and preparation methods and uses thereof 4-Hydroxyquinoline-3-amide derivatives represented by formula I, isomers, racemates, optical isomers, pharmaceutical salts or solvates thereof are disclosed, wherein X, Y, R1-R5 are defined as in the description. The preparation methods for said compounds, the compositions containing said compounds and uses thereof in the manufacture of medicaments for preventing and/or treating autoimmune diseases and/or disorders relevant to immune system functional disorders are also disclosed.
US20120269761 Biodegradable elastomers The present inventions in various aspects provide elastic biodegradable polymers. In various embodiments, the polymers are formed by the reaction of a multifunctional alcohol or ether and a difunctional or higher order acid to form a pre-polymer, which is cross-linked to form the elastic biodegradable polymer. In preferred embodiments, the cross-linking is performed by functionalization of one or more OR groups on the pre-polymer backbone with vinyl, followed by photopolymerization to form the elastic biodegradable polymer composition or material. Preferably, acrylate is used to add one or more vinyls to the backbone of the pre-polymer to form an acrylated pre-polymer. In various embodiments, acrylated pre-polymers are co-polymerized with one or more acrylated co-polymers.
WO2010122064A1 Substituted naphthyridine derivatives and their medical use The present application discloses novel substituted naphthyridine derivatives of Formula (I) and their use as modulators of the voltage gated Kv7 (KCNQ) potassium ion channels.In other aspects the application discloses the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising these compounds.
US20060142235 Method of reducing and treating UVB-induced immunosuppression Methods of preventing and/or treating UV-induced immunosuppression by administration of immune response modifier compounds are disclosed herein. Suitable immune response modifier compounds include agonists of one or more TLRs.
US20090042918 Pyridopyrimidinone Inhibitors of PIM-1 and/or PIM-3 Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R1, R3, Q, X and R4 are as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed.
CN101759695A Thiazole derivative containing pyrazole ring and preparation method and application thereof The invention relates to a thiazole derivative containing a pyrazole ring, comprising the following general formula: in the formula: R3 = F, Cl, Br, CH3, OCH3, OH or NO2; R4=C1 or H; when R1=CH3, R2=CH3; and when R1=Br, R2=H. The novel thiourea derivative containing the pyrazole ring has a significantly inhibited role for a human oral epithelial cell line (KB) and a human leukemia cell line (K562), so the thiourea derivative can be applied to the preparation of anticancer drugs. The invention discloses a preparation method of the thiourea derivative.
US20090074863 Dosage Forms Containing A PPI, NSAID And A Buffer Provided herein, are dosage forms comprising an NSAID, a buffer and a PPI, as well as methods of treating various maladies using the above dosage form.
WO2011136318A1 Therapeutic agent and preventative agent for alzheimer's disease Disclosed are a therapeutic agent and preventative agent for Alzheimer's disease having an inhibiting or delaying action on the progress of Alzheimer's disease and maintaining a therapeutic effect on Alzheimer's disease even with long-term administration. Specifically disclosed are a therapeutic agent and preventative agent for Alzheimer's disease that contain a cyclohexane derivative represented by the formula, a pharmacologically acceptable salt thereof, or a prodrug thereof as the active ingredient.
US20120251616 Tocopherols, Tocotrienols, Other Chroman and Side Chain Derivatives and Uses Thereof The present invention provides an antiproliferative compound having a structural formula where X and Y independently are oxygen, nitrogen or sulfur; R1 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxylic acid, carboxylate, carboxamide, ester, thioamide, thiolacid, thiolester, saccharide, alkoxy-linked saccharide, amine, sulfonate, sulfate, phosphate, alcohol, ethers or nitriles; R2 and R3 are hydrogen or R4; R4 is methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide or amine; and R5 is alkenyl; where when Y is nitrogen, said nitrogen is substituted with R6, wherein R6 is hydrogen or methyl. Also provided are methods for treating a cell proliferative disease and for inducing apoptosis in a cell comprising administering this compound is also provided.
CN102743443A Compound glycyrrhiza oral solution preparation technology The invention discloses a compound glycyrrhiza oral solution preparation technology which comprises the following steps: preparing extractum glycyrrhizae liquidum with pH value of 8.5, 25% alcohol in volume fraction and the glycyrrhizic acid content conforming to the specification; weighing camphor, opium tincture, star anise oil, ethanol, extractum glycyrrhizae liquidum, glycerol, guaifenesin, strong ammonia solution, benzoic acid and sodium sulfite; and preparing compound camphor tincture for later use. The compound glycyrrhiza oral solution is prepared by the following steps: adding the weighed extractum glycyrrhizae liquidum and glycerol into a dispensing pot; stirring and mixing evenly; adding purified water for dilution; sequentially and slowly adding the sodium sulfite solution, the guaifenesin water solution and the compound camphor tincture solution, and stirring while adding; adding purified water to 98% of the prepared amount, regulating the pH value to be 8.00-8.20 with the strong ammonia solution, and stirring while adding; then adding purified water to a constant volume of the needed preparation amount; and filling and packaging to obtain finished products after the inspection is passed. Therefore, the quality and stability of products can be improved, and the curative effect is enhanced.
CN102973665A Toothache treatment buccal tablet and preparation method The invention discloses a toothache treatment buccal tablet and a preparation method. The preparation method comprises the following steps: (1) weighing long pepper, clove and borneol; (2) conducting reflux extraction on the long pepper with an ethanol water solution, filtering, recovering ethanol from the filtrate to obtain a thick extract, adding the ethanol water solution, mixing uniformly, standing, and conducting vacuum condensation to obtain an extract 1; (3) extracting clove oil from the clove by a steam distillation method to obtain an extract 2; (4) drying and crushing the extract 1, mixing the dried and crushed extract 1 with the extract 2 and the borneol, adding a lubricating agent and a corrigent, mixing, and then tableting to form the toothache treatment buccal tablet. The toothache treatment buccal tablet prepared by the preparation method takes effects quickly, is convenient to take, has remarkable treatment effect, and can address both the symptoms and the root causes, so that the requirements of the majority of patients are met. According to the preparation method, the labor hour is short, and the transfer ratio of active ingredients is high.
WO2009145719A1 Isoindoline derivatives comprising a cyano group and their use in the treatment of pain disorders Compounds of formula I are claimed, wherein R1 is hydrogen, C1_3alkyl, C1_3alkoxy, cyano, hydroxy or halo; and wherein said C1-3alkyl is optionally substituted by one or more substituents independently selected from hydroxy, C1_3alkoxy andfluoro; and said C1_3alkoxy is optionally substituted by one or more fluoro; m is 1, 2 or 3; R2 and R3 is each and independently selected from hydrogen, C1-4haloalkyl, C1-4haloalkoxy, halo, C1-4alkoxy, C1-4alkyl and C3_7Cycloalkyloxy; wherein said C3_7cycloalkyloxy is optionally substituted by one or more fluoro; and R2 and R3 may not both be hydrogen; L1 is C1-4alkylene, pentylene, or C3-6 cycloalkylene, wherein said C1-4alkylene, pentylene or C3-6 cycloalkylene may be optionally substituted by one or more X4; X4 is fluoro, C1_3alkyl, C3_7Cycloalkyl, C1_3alkylOCi_3alkyl, C1_3alkoxy, cyano, hydroxy, R4O(C=O)-, R4NR5(C=O)-, R4O(C=O)NR5-, R4NR5(C=O)NR5-, R4(C=O)O-, R4(C=O)NR5-, R4NR5(C=O)O-, R4NR5(C=O)NR5-, C5-6 heteroaryl(C=O), or C5-6 heteroaryl; R4 is C1-4 alkylOC1-4 alkyl, C5-6 cycloalkyl, aryl, or aryl-C1-2 alkyl; R5 is H or methyl; and wherein said C1-3 alkylOC1-3alkyl, C1-3alkoxy and C1-4alkylsulfonyl is optionally substituted by one or more fluoro; L2 is C1-3 alkylene, optionally substituted by one or more X4; as well as pharmaceutically acceptable salt, or isomer thereof, or a salt of said isomer. Compounds of the invention are useful in therapy, such as pain therapy.
CN102872009A Application of Eryngiolide A in drugs for inhibiting liver fibroblast cell proliferation The invention discloses an application of Eryngiolide A in preparing drugs for treating liver fibrosis. Proved by pharmacological testing, the Eryngiolide A is capable of obviously inhibiting the occurrence and the development of liver fibrosis. The Eryngiolide A can be used for preparing the drugs for resisting the liver fibrosis and preventing and curing cirrhosis. The application of the Eryngiolide A in preparing the drugs for inhibiting liver fibroblast cell proliferation is disclosed for the first time. As the skeleton type of the Eryngiolide A is fire-new, and moreover, how high the activity of the Eryngiolide A inhibiting the liver fibroblast cell proliferation is unexpected, the possibility that any enlightenments are given by other compounds does not exist. The Eryngiolide A has outstanding substantive features, and meanwhile, apparently achieves a significant progress when being used for resisting the liver fibroblast cell proliferation.
EP1280897B1 Regulation of nf-at interacting protein nip 45 variant Disclosed are novel nucleic acid and amino acid sequences of NF-AT interacting protein NIP 45 variants. Reagents that bind to NIP45-variant gene products can be used to treat conditions involving inflammatory processes, such as allergy, asthma, autoimmune diseases, and other chronic inflammatory diseases where an over-activation or prolongation of the activation of the immune system causes damage to tissues.
EP1104309B1 Co-lyophilized complex comprising a nucleic acid vector and a formulating agent The present invention, as noted above, relates generally to the incorporation of plasmid into a conventional dosage form, and more particularly to the production of a single-vial, homogenized, plasmid/polymer complex with desirable physical characteristics. Methods of making, storing and using such a complex are also provided and described in detail below. Such products and methods will provide more convenient and cost-effective complexes, which will be protected against chemical degradation and/or physical aggregation of its components and will provide for relative ease of administration. Thus, the present invention provides a more efficient complex for plasmid delivery and a method of incorporation of that plasmid into a conventional dosage form.
US20080108647 Treatment of HIV and diseases of immune dysregulation This invention discloses cannabinoid derivatives and pharmaceutical uses thereof including the treatment of HIV and diseases of immune dysregulation.
US20080058410 Composition for Stabilizing Vitamin C in Water Phase and Method for Stabilizing C Using Thereof The present invention relates to a composition for stabilizing vitamine C in water phase and method for stabilizing vitamine C using the composition. More particularly, this invention relates to a composition wherein the vitamine C is effectively prevented from decomposing by an exterior environment such as water, temperature, and light by stabilizing the vitamine C with the use of a cationic polymer and an anionic polymer, and thereof method for stabilizing vitamine C.
WO2007086457A1 Quickly disintegrating tablet produced by direct dry-tabletting It is intended to provide a quickly disintegrating tablet, which has a practically appropriate tablet hardness while sustaining the disintegrability, and a process for producing the same by the direct dry-tabletting method wherein a material mixture powder before tabletting has a high flowability owing to well designed combination of an active ingredient with auxiliary ingredient(s) and, therefore, can be smoothly flown out from the hopper of a tabletting machine, no capping occurs during tabletting and the obtained tablets show little deviation in weight. Namely, a quickly disintegrating tablet produced by the direct dry-tabletting method characterized by containing (a) an active ingredient and (b)as a dissolution aid, at least one member selected from the group consisting of acid selected from among citric acid, tartaric acid, malic acid, lactic acid and ascorbic acid or alkali metal salts thereof; alkali metal hydrogencarbonates; and alkali metal carbonates, together with (c) a filler, (d) a binder, (e) a disintegrating agent, (f) a fluidizer, and (g) as a lubricant, a lubricant comprising a combination of magnesium stearate with a sucrose fatty acid ester.
CN101239066A Triamcinolone acetonide econazole cream The invention discloses a triamcinolone acetonide and econazole nitrate cream which contains econazole nitrate and triamcinolone acetonide. The invention is characterized in that the cream also contains octodecyl alcohol or hexadecanol. The triamcinolone acetonide and econazole nitrate cream is more subtle and even, is easy to be daubed and washed on and away from the skin and is harmless to skin, has no odor. No greasiness is to be felt when the cream is daubed on the skin, and the quality is more stable.
WO2014071355A1 1,3,4-oxadiazoles-2-thio azetidine derivatives as sphingosine-1 phosphate receptors modulators The present invention relates to substituted 1,3,4-oxadiazoles-2-thio azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
CN102048698A Streptomycin sulfate albumin microspheres and preparation method The invention relates to streptomycin sulfate albumin microspheres and a preparation method. The streptomycin sulfate albumin microspheres are nearly suitable for various administration paths such as intravenous injection, intramuscular injection, oral administration, mucosal administration, administration in joint cavities and the like. The microsphere preparation has obvious release controlled effect, and can prolong the acting time of medicaments, improve bioavailability and reduce adverse reaction. When the medicaments fulfill targeted purpose, many biological barriers such as blood brain barriers, dermis, netlike endothelial systems and bio-membrane systems of pathogens in organisms can be overcome. Through the properties of the streptomycin sulfate albumin microspheres, the medicaments can generate effective and reliable targeted effect in the organisms.
US20120288534 Corticosteroids for the Treatment of Joint Pain Corticosteroid microparticle formulations are provided for use for treating pain, including pain caused by inflammatory diseases such as osteoarthritis or rheumatoid arthritis, and for slowing, arresting or reversing structural damage to tissues caused by an inflammatory disease, for example damage to articular and/or peri-articular tissues caused by osteoarthritis or rheumatoid arthritis. Corticosteroid microparticle formulations are administered locally as a sustained release dosage form (with or without an immediate release component) that results in efficacy accompanied by clinically insignificant or no measurable effect on endogenous cortisol production.
US7064136 Central nervous system disorders; psychological disorders; schizophrenia; antiarthritic agents; Alzheimer's disease; anticancer agents A compound having the general formula and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
WO2014110261A1 Cyp450 lipid metabolites reduce inflammation and angiogenesis Methods for reducing angiogenesis, inflammation, and vascular permeability in a subject by administering an epoxymetabolite of Docosahexaenoic acid (DHA) and Eicosapentaenoic acid (EPA), e.g., as listed in Table A, e.g., one or both of 17,18- epoxyeicosatetraenoic acid (EEQ) and 19,20-epoxydocosapentaenoic acid (EDP), e.g., for the treatment of conditions associated with inflammation or excess angiogenesis or neovascularization, including age-related macular degeneration, cancer, stroke, and arthritis.
US20080058312 Modulators of hepatocyte growth factor/c-Met activity This invention is directed to compounds and compositions that have biological properties useful for modulating HGF/SF activity. In certain embodiments, said compounds and compositions may be used in the treatment and prophylaxis of cancer or other dysproliferative diseases and inflammatory diseases such as rheumatoid arthritis.
CN101829115A Application of chloroquine compound or salt thereof in preparation of medicament for treating acute leukemia The invention provides an application of a chloroquine compound or a salt thereof in the preparation of a medicament for treating acute leukemia. The chloroquine compound or the salt thereof can be any one of chloroquine, chloroquine phosphate, hydroxychloroquine, chloroquine hydrochloride, nivaquin, chloroquine silicate or aminochloroquine. By using the chloroquine medicament having stabilizing effect on the cell membrane and the intra-cellular membrane structure to treat the leukemia cell strain and the primary cell, the growth of the leukemia cell can be retarded and the apoptosis rate of the leukemia cell can be obviously increased after the treatment, thereby indicating that the chloroquine compound and the salt thereof can be used for treating leukemia.
US20080039434 Treatment of Interstitial Cystitis with Vitamin D Compounds There is provided according to the invention a vitamin D compound for use in the prevention and/or treatment of interstitial cystitis. Also provided is a method for preventing and/or treating interstitial cystitis by administering an effective amount of a vitamin D compound.
US20100035998 Combination s-nitrosothiol pharmaceutical products for restoring normal breathing rhythms The present invention is directed to a method of treating a lack of normal breathing control including the treatment of apnea and hypoventilation associated with sleep, obesity, certain medicines and other medical conditions. In an aspect, the invention is directed to treating disordered control of breathing by administering an composition comprising a combination of two or more compounds, at least one of which treats lack of normal breathing. In one aspect, a compound is an S-nitrosylating agent.
CN102240274A Application of magnolol and honokiol in protein tyrosine phosphatase 1B inhibitor The invention relates to application of magnolol and honokiol in a protein tyrosine phosphatase 1B inhibitor, belonging to the technical field of tyrosine phosphatase inhibition. The magnolol and honokiol provided by the invention are natural products extracted from Magnolia used as the raw material; and in-vitro experiments show that the magnolol and honokiol can inhibit the biological activity of human protein tyrosine phosphatase 1B, can be used for the adjuvant treatment of the related diseases caused by (protein tyrosine phosphatase 1B), and thus the magnolol and honokiol can be used for preparing the food, medicaments or food and medicament compositions for the treatment and prevention of the diseases related to the overhigh activity or over-expression of protein tyrosine phosphatase 1B.
CN101712594A 2-cyclohexyl-5-(1,1- dimethyl octyl) phenol and synthesizing method thereof The invention relates to a 2-cyclohexyl-5-(1,1-dimethyl octyl) phenol and a synthesizing method thereof. 2-benzyloxy-1-bromine-4-(1,1-dimethyl octyl) benzene carries out addition reaction to obtain 2-benzyloxy-1-(cyclohexyl or 3'-alkoxy cyclohexyl)-4-(1,1-dimethyl octyl) benzene, and the 2-benzyloxy-1-(cyclohexyl or 3'-alkoxy cyclohexyl)-4-(1,1-dimethyl octyl) benzene is hydrogenated to carry outbenzyl removing reaction to obtain the 2-cyclohexyl-5-(1,1-dimethyl octyl) phenol. The invention has short synthesizing route, simple method and higher yield and is easy for industrialized production. The 2-cyclohexyl-5-(1,1-dimethyl octyl) phenol has liquid crystal performance and excellent antibiosis inflammation eliminating effect, can be used as one of liquid crystal composition components ofa liquid crystal display, has the inhibiting effect on porphyromonas gingialis, streptococcus, spider-shaped selenomonas, and the like and can be used for preparing a mouth cleaning agent and a medicament for preparing oral cavity diseases.
US6903132 Non-peptide GnRH agents, pharmaceutical compositions and methods for their use Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
US7608618 1-(2,2,2-trifluoroethanoyl)pyrrolidine-2-carboxylic acid [4-methoxy-3-(3-pyrazin-2-yl-ureido)phenyl]-amide; 4-Methoxy-N-(3-methylamino-propyl)-3-(3-pyrazin-2-yl-ureido)-benzamide; checkpoint kinase Chk1 inhibitor; chemosensitizing agents useful in the treatment of diseases related to DNA damage Compounds of the formula wherein: Y′ is O or S, W′ is optionally substituted, Z′ is selected from the group consisting of wherein Q′ is OR7 and R7 is C1-3alkyleneC3-8heterocycloalkyl useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.
US20110263699 1-Phenyl-2-DimethylaminomethylCyclohexane Compounds and Therapies for Depressive Symptoms, Pain and Incontinence Metabolites of [2-(3-methoxyphenyl)-cyclohexylmethyl]dimethylamine as free bases and/or in the form of physiologically acceptable salts, corresponding medicaments, the use of [2-(3-methoxyphenyl)-cyclohexylmethyl]-dimethylamine and the metabolites thereof for producing a medicament used for treating depression, and related methods of treating depression, pain and urinary incontinence.
WO2007059952A3 1-benzazepine-3-sulfonylamino-2-pyrrloridones as factor xa inhibitors The invention relates to chemical entities of formula (I): and/or pharmaceutically acceptable derivative(s) thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
US20110262542 Controlled Delivery of Tetracycline Compounds and Tetracycline Derivatives A composition is provided for delivering a tetracycline compound to a mammal. The composition includes an antibiotic tetracycline compound and a controlled-release agent having at least one controlled-release agent. The tetracycline compound is associated with the controlled-release matrix to provide a release profile whereby the mammal is treated substantially without antibiotic activity. Methods for treating a mammal with a tetracycline compound and a dosage unit are also provided utilizing the controlled-release tetracycline composition.
US20090131539 Mixture A mixture of substances, in particular a biocide for combating human and animal parasites comprising a) an A component containing at least one type of alcohol of general formula R1-OH or R1-OH—R1′, wherein R1 and/or R1′ is an alkyl radical associated with a hydroxyl group which comprises from 1 to 12, preferably from 1 to 6, carbon atoms, b) a B component consisting of at least one type of carbonyl compound of formula R2-CO—R2′, wherein R2 and/or R2′ is an aryl-, alkyl- or cycloalkyl radical associated with a carbonyl group containing from 1 to 5, preferably from 1 to 2, carbon or hydrogen atoms, and c) at least one type of essential oil in the form of a C component consisting of an aromatic hydroxy compound of formula R3-0H, wherein R3 is a compound of at least one type of cyclic aryl radical which can be substituted up to two times and at least one organic compound R3′, wherein R3′ is an aryl-, alkyl- or cycloalkyl radical, wherein the components A and B are brought into reaction with hydrogen peroxide and the component C is subsequently mixed.
CN102657647A Application of IC-4 in antiangiogenesis The invention discloses an application of a compound IC-4 with the structural formula represented by formula (I) or its salts in antiangiogenesis, and further discloses an application of the compound IC-4 with the structural formula represented by formula (I) or its salt in preparation of antiangiogenic agents. Researches on the application of the IC-4 or its salt in the antiangiogenesis are based on researches on growth factor induced endothelial cell growth inhibition, angiogenesis inhibition, endothelial cell migration inhibition and endothelial cell transfer inhibition of the IC-4 or its salts, and combine with a scientific and reasonable research system constructed through integral experiments of zebra fish embryo angiogenesis.
US7635693 Methods for preventing and treating cancer using N-thiolated β-lactam compounds and analogs thereof The subject invention concerns N-thiolated β-lactam compounds of formula A, wherein R1 is a hydrocarbon group having 1-8 carbon atoms; R3 is an organothio group; and R4 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, and analogs and pharmaceutically acceptable salts, esters and amides thereof. The subject invention also concerns methods for inducing tumor cell death or inhibiting tumor cell proliferation, and methods for inducing DNA damage, inhibiting DNA replication, activating p38 MAP kinase, or activating caspase cascade activation, or releasing cytochrome C from mitochondria into the cytoplasm in a tumor cell. Methods for treating cancer using N-thiolated β-lactam compounds, as well as pharmaceutical compositions comprising the same are further disclosed.
WO2007053194A3 Modulation of cell barrier dysfunction The invention provides prophylactic and therapeutic methods for administering a μ-opioid receptor antagonist to treat cell barrier diseases and disorders, such as endothelial and epithelial cell barrier diseases and disorders. The diseases or disorders may amenable to the methods include inflammation, such as acute lung injury, atherosclerosis, gut-derived sepsis, a burn injury, neonatal necrotizing enterocolitis, severe neutropenia, toxic colitis, inflammatory bowel disease, enteropathy, transplant rejection, pouchitis, pig belly (pig-bel), Pseudomonas-mediated ophthalmologic infection, Pseudomonas-mediated otologic infection and Pseudomonas-mediated cutaneous infection. More generally, epithelial cell barrier disorders are contemplated as amenable to the prophylactic and therapeutic methods.. The diseases and disorders may be induced by microbial pathogens, including bacterial pathogens such as Pseudomonαs aeruginosa. The invention further provides prophylactic and therapeutic methods for inhibiting the expression of bacterial PA-I lectin/adhesin and for inhibiting bacterial MvfR activity levels. Also provided is a method of using a μ-opioid receptor antagonist in the manufacture of a medicament for use in the methods described herein.
CN102250047A More-stable taxol compound and medicament composition thereof The invention relates to a taxol compound and a medicament composition thereof. In a preparation method of the more-stable taxol compound, rough taxol is re-crystallized 1-3 times by utilizing a mixed solvent composed of cyclohexane and acetone in the ratio of 2 to 1; meanwhile, the crystal is de-colored by using active carbon to obtain a white crystal, wherein the ratio of the rough taxol to the mixed solvent is 1 to 10 and the use amount of the active carbon accounts for 5% of the volume of the solution.
WO2012016162A2 Compositions, methods and kits for modeling, diagnosing, and treating complement disorders Systems, compositions, methods, and kits for identifying potential therapeutic agents for treatment of complement based ocular diseases are provided herein. The methods and kits include a complement component 3 (C3) protein or derivative that is contacted to ocular cells or tissue. Another embodiment of the invention herein provides for diagnosis and/or prognosis of a complement-associated ocular disease. Compositions, methods and kits for regulating or treating a complement-related condition using at least one of CD46 protein, CD55 protein, and a recombinant chimeric soluble terminator of activated complement (STAC) protein or source of the STAC protein. The STAC protein includes an amino acid sequence including at least two of an amino acid sequence of a CD59 protein, an amino acid sequence derived from a CD46 protein, and an amino acid sequence derived from a CD55 protein, optionally further comprising a linker to connect amino acid sequences.
US6919347 Antidiabetic agents; antiinflammatory agents; analgesics; antiallergens Bradykinin B1-receptor antagonists of formula are disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflammation, pain, hyperalgesia, asthma, rhinitis, septic shock, atherosclerosis and multiple sclerosis. Pyrimidines, triazines, and anilines in which Q is imidazolyl or pyrrolyl are particularly preferred.
CN101057869A Pearl eyesight instant gel for eye The invention discloses an instant pearl gel for improving acuity of vision and process for preparation, wherein each 1000ml of the gel comprises pearl liquid 10-30ml, borneol 0. 8-1. 5g, preservative agent 0. 05-1g, osmoregulation agent 10-75g, gel base material 30-150g, balancing acid-alkali buffering agent and water for injection.
WO2010084120A1 N-oxides of 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives useful as nicotinic acetylcholine receptor ligands This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein Ar represents an indolyl group, which indolyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, triflυoromethoxy, cyano, nitro, amino, alkyl, hydroxy and alkoxy.
CN101152191A Lotepredenol etabonate gernebcin suspension solution and method for preparing the same The invention discloses an eye use compound drug combination containing lotepredenol etabonate and tobramycin. The combination contains less than 0.1 percent of tetra chloro metlbond. The preparation method of the drug combination is simple and is suitable for industrial production.
WO2011143444A3 Diphenylbutypiperidine autophagy inducers Autophagy inducing compounds, methods of their preparation and use, and kits containg said compounds are disclosed herein.
WO2008086330A3 Formulations of deacetylase inhibitors The present invention provides a stable parenteral formulation of histone deacetylase inhibitors.
US20120295899 Benzylpyrrolidinone derivatives as modulators of chemokine receptor activity The present application describes modulators of MCP-1 or CCR-2 of formula or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, W, X, R1 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
US20090062388 Use of acetyl L-carnitine for the preparation of a medication for the preventive therapy for pain The invention relates to the use of the acetyl L-carnitine, or a pharmaceutically acceptable salt thereof for the preparation of a medication for the preventive therapy for pain.
US20110262552 Compositions Comprising Plant Extracts and Use Thereof for Treating Inflammation Provided are compositions comprising Harpagophytum procumens (Devil's claw) root extract and Ribes nigrum (Black Currant) leaf or seed extract. Other components may also be included. Also provided are methods of preventing or treating inflammation or a condition that results from inflammation.
CA2153348C Enteral diet and method for providing nutrition to a diabetic A composition and method for providing nutrition, or a nutritional supplement, to a diabetic patient. Pursuant to the present invention, a low carbohydrate, high fat enteral formulation is provided. The fat comprises, in part, medium chain triglycerides (MCTs). Preferably, the composition includes a high percent of mono-unsaturated fats, high amylose starch, and soluble dietary fiber.
US7585878 2-[(2,5-dimethylpyrrolidin-1-yl)methyl]-N-(1-methyl-2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)biphenyl-4-carboxamide; capsaicin receptor VR1 inhibitory activity; inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like. A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).
CN103041390A Melbine and ezetimibe combined composition medicament for treating nonalcoholic fatty liver disease The invention relates to a medicinal composition. The medicinal composition comprises a melbine hypoglycemic medicine, cholesterol adsorption and inhibition ezetimibe and a medicinal vector, wherein the melbine hypoglycemic medicine is selectively in a pharmaceutically acceptable salt form. The medicinal composition is suitable for treating nonalcoholic fatty liver disease.
WO2007149557A1 FUSED [d]PYRIDAZIN-7-ONES The present invention is directed to fused [d] pyridazin-7-ones of formula (I). The invention is also directed to methods for making and using the fused [d] pyridazin-7-ones. In particular, the compounds of the present invention may he effective in the treatment of diseases or disease states related to the activity of VEGFR2, MLKl and CDK5 enzymes, including, for example, angiogenic disorders and neurodegenerative diseases.
CN103087040A Penicillide derivative, preparation method thereof, and medicinal purpose thereof The invention belongs to the field of medicine synthesis, and specifically relates to a novel penicillide derivative, a preparation method thereof, a medicine composition comprising the derivative, and a purpose thereof as a therapeutic agent. The penicillide derivative provided by the invention is a compound with a general formula (I). The penicillide derivative provided by the invention can be used as an effective component for preparing a medicine composition and especially a cholesterol esters transfer protein inhibitor. R1 is selected from (1R,4S)-7-methylbicyclo[2.2.1]heptane-7-carbony, 4-bromobenzoyl, 4-trifluoromethyl benzoyl, and 3,5-di(fluoromethyl)benzoyl; R2 is selected from hydrogen, methyl, and p-methoxyphenyl; and R3 is selected from hydrogen, and methoxy.
CN101277956A Imidazo [1,2-A] pyridine having anti-cell-proliferation activity Compounds of formula (I) which possess cell cycle inhibitory activity are described.
EP1285908B9 Substituted phenylpropionic acid derivatives Novel substituted phenylpropionic acid derivatives of the general formula (1), which bind to human peroxisome proliferator activated receptor alpha (PPAR alpha ) as ligand to activate the receptor and thereby exhibit a potent lipid-decreasing effect; and use thereof as drugs: (1) wherein R<1> is lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, optionally substituted phenyl, optionally substituted phenoxy, or optionally substituted benzyloxy; R<2> is hydrogen, lower alkyl, or lower alkoxy; R<3> is lower alkoxy; and A is -CH2CONH-, -NHCOCH2-, -CH2CH2CO-, CH2CH2CH2-, -CH2CH2O-, -CONHCH2-, -CH2NHCH2-, -COCH2O-, -OCH2CO-, -COCH2NH-, or NHCH2CO-.
CN103463100A Application of Kadcoccitones A in preparing medicament for reducing blood sugar The invention discloses application of Kadcoccitones A in preparing a medicament for resisting diabetes mellitus. Kadcoccitones A is proved to have a remarkable diabetes mellitus resistance effect. Kadcoccitones A is a compound with a definite chemical structure, belongs to a brand-new frame model, has a strong activity for preventing and treating diabetes mellitus, has a highlighted substantial characteristic, and is remarkably progressed when being used for resisting diabetes mellitus.
CN101394851A Gsk-3 inhibitors for the treatment of osteoporosis The present invention relates to a new use of a compound of the formula (I) wherein R1 is NH2, piperazin-1-yl, 4-methylpiperazin-1-yl, 4-methyl-1,4-diazepan-1-yl or 4-ethylpiperazin-1-yl; R2 is hydrogen, fluoro, CH3, CH2CH3, OCH3, CF3 or OCF3; R3 is hydrogen, CH3 or fluoro; as a free base or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the prevention and/or treatment of bone-related disorders, osteoporosis and increasing bone formation, bone mineral density. The present invention further relates to a method of prevention and/or treatment of these disorders.
US7067635 For use in diagnostic methods, immunotherapy, gene therapy and as vaccines The present invention discloses the isolation of the human and murine wild-type Int6 gene and the cDNAs sorresponding to these genes. The invention further describes the use of reagents derived from the nucleic acid and amino acid sequences of the Int6 gene in diagnostic methods, immunotherapy, gene therapy and as vaccines.
US20120157467 Composition and use for phosphodiesterase inhibitors Compositions and methods for enhancing the aesthetic appearance of the lip or lips of a human achieved by applying to the surface of the lip a composition containing a phosphodiesterase inhibitor, preferably a pyrazolopyrimidinone such as sildenafil or its citrate salt.
CN101543632A Anti-tumor prodrug having accurate structure and taking novel amphipathic polymer as carrier and synthetic method thereof The invention discloses a prodrug system prepared by connecting a series of oligopolymers synthesized by a group protection and deprotection method and polyethyleneglycol to be used as a drug carrier, belonging to the technical field of chemical drugs. Laden drugs are water-insoluble anti-tumor drugs such as taxol, or other cancer therapy drugs such as doxorubicine and camptothecin. A research discovers that drug compositions prepared by the method greatly improve the hydrophobic nature of the anti-tumor drugs and can accurately control the gather time of the oligopolymers on focus parts and the hydrolyzation rupture time of ester bonds by accurately controlling the lengths of segmers of the oligopolymers so as to control the drug release time so that drugs are stably released, thereby the method prevents burst release causing toxic side effect on normal cells, reduces the drug dosage to enhance the curative effect and sufficiently plays a sustained and controlled release role; and in addition, the structure of the oligopolymers is accurate, and the molecular weight of synthesized amphipathic block polymers which are uniformly distributed is accurate, thereby the method can ensure synthesized drug ingredients to be definite and stable and the pharmacokinetics and the treatment effect (activity and toxicity) of the synthesized drugs to have good reproduction quality and be accurately defined.
CN101407517B Preparation of ambroxol theophylline-7-acetate The invention provides a method for preparing ambroxol theophylline-7-acetate and belongs to the field of chemical medicine. The method takes water, ethanol or methanol as a solvent, the theophylline-7-acetic acid and ambroxol alkali react with the weight ratio of 1 to 1.49 to 1.69, and the ambroxol theophylline-7-acetate is prepared, and the ratio of the theophylline-7-acetate and the solvent byweight ratio is 1 to 20 to 60. The steps of the method are simple, the content of the obtained ambroxol theophylline-7-acetate is more than 98 percent, and the weight yield rate is more than 113.0 percent calculated in ambroxol alkali. As taking water as the reaction solvent, the method has the advantages of low cost, easy recovery and treatment and reducing the pollution of organic solvent emission to the environment.
US20100130596 Rad51 derived cancer cell specific promoters for targeted anti- cancer therapy Provided are compositions and methods for inhibiting growth of cancer cells. The method of the invention relates to delivering to cells an effective amount of a composition that contains a polynucleotide having a Rad51 promoter or a polynucleotide having at least 95% similarity to a Rad51 promoter. The Rad51 promoter is operably linked to a coding region for a cytotoxic agent. In vitro and in vivo results demonstrating effectiveness of the polynucleotides of the invention are presented.
CN103463060A Application of Lycojaponicumin C in preparation of medicines for treating endometrial cancer The invention discloses an application of Lycojaponicumin C in the preparation of medicines for treating endometrial cancer, belonging to the technical field of new applications of medicines. The evaluation on an in vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anti-tumor activity shows that the Lycojaponicumin C also has an obvious inhibiting effect on the growth of human endometrial cancer cell lines ISK and RL95-2. Therefore, the Lycojaponicumin C can be used for the preparation of the medicines for resisting the endometrial cancer and has good development and application prospects. The application of the Lycojaponicumin C in the preparation of the medicines for treating the human endometrial cancer is disclosed for the first time. As the skeleton type of the Lycojaponicumin C belongs to a brand-new skeleton type, the Lycojaponicumin C has unexpected strong inhibitory activity on endometrial cancer cells.
WO2013085957A1 Substituted piperidinyl-pyridazinyl derivatives useful as scd 1 inhibitors The present invention is directed to novel piperidinyl-pyridazinyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.
CA2840222A1 Compositions and methods for treating skeletal myopathy The present invention provides a method of preventing or treating a myopathy, such as a skeletal myopathy, comprising administering a modulator of a miRNA. In one embodiment, the skeletal myopathy is centronuciear myopathy. The modulator can be an agonist that promotes the expression, function or activity of a miR-133 family member. The miR-133 family member can be miR-133a or miR-133b.
US7534803 Potassium and sodium channel moderators; brain disorders; strokes; multiple sclerosis N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.
CN101332192A Preparation of nifuratel and nysfungin vaginal soft capsules The present invention relates to preparation of a new medicine Nifuratel nysfungin vagina tablet for gynecologic antisepsis and anti-inflammation. Nifuratel nysfungin can play a more complete role in curing mixed vagina infection (candida, trichomonas and bacteria) and pathogen which can not be or can not be timely and clearly diagnosed and preventing mildew secondary infection and recurrence after the treatment of other medicines. The present invention can be used for curing bacterial vaginopathy, trichomonas vaginitis, monilial vulvovaginitis, and vagina mixed infection. The advantage of the present invention lies in that the added pH buffer system ensures pH of the medicine is within 3.5 to 4.0 close to the physiological pH of vagina, thus effectively protecting the physiological environment of vagina, providing the appropriate living conditions beneficial to flora in vagina and promoting the recovery of diseases.
CN102895219A Application of astaxanthin in fetal alcohol spectrum disorders (FASD) The invention discloses an application of astaxanthin in preparing a drug for treating fetal alcohol spectrum disorders (FASD). The astaxanthin not only is capable of effectively inhibiting embryonic development lag and oxidative stress index increase which are caused by alcohol but also is capable of resisting the reduction of alcoholic neurodevelopment markers. The astaxanthin is a compound capable of effectively interrupting the FASDs. Discovered for the first time in experiments that toll-like receptors (TLRs) participate in the development of the FASDs, the astaxanthin is capable of reducing the expression of TLR4-messenger ribonucleic acid (mRNA) in an embryonic body because of the alcohol, inhibiting the expression level of TLR4 and the expression level of the downstream protein of the TLR4 and reducing the inflammatory factor increase caused by the alcohol. A new way is provided by the invention for preventing and treating the fetal alcohol-related disease.
WO2007143823A1 Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I)
CN103263412A Bionic antibacterial anti-inflammatory agent The invention discloses a bionic antibacterial anti-inflammatory agent which is alpha-R base-gamma-methylene-gamma butyrolactone. The structural formula of the alpha-R base-gamma-methylene-gamma butyrolactone is as follows: R is an alkyl chain, an alkenyl chain or an alkynyl chain. By adopting the mode, the bionic antibacterial anti-inflammatory agent provided by the invention is derived from natural substances, has structural specificity, can be used for effectively solving and curing or relieving the skin problem and disease which are caused by malassezia, has the advantages of safety, high efficiency, high sterilization efficiency, good heat stability and low cost, is an antibacterial anti-inflammatory agent almost without burden on the environment and can be applied to large-scale pharmaceuticals and daily chemical articles.
US20080044488 Nano Glass Powder and Use Thereof, in Particular Multicomponent Glass Powder with a Mean Particle Size of Less Than 1 µm A glass powder or a glass-ceramic powder is provided that includes multicomponent glasses with at least three elements, where the glass powder or a glass-ceramic powder has a mean particle size of less than 1 μm. In some embodiments, the mean particle size is less than 0.1 μm, while in other embodiments the mean particle size is less than 10 nm.
CN101463015B Preparation of 5,6,7-trialkoxy-N-aryl substituted-4-amino quinazoline derivative and compound synthesized thereby The invention provides a preparation method of 5,6,7-trialkoxy-N-aryl-substituted-4-aminoquinazoline derivatives and compounds which are synthesized by the method, and discloses a method which is characterized by taking 2,3,4- trialkoxy benzoic acid, nitric acid, methanol, sulfuric acid, iron powder, ammonium chloride, sodium, formamide, phosphorus oxychloride, triethylamine and aromatic amine asraw materials, taking the methanol, ethanol, isopropyl alcohol, N,N-dimethyl formamide and toluene as solvents, and synthesizing by six steps. The method is characterized by introducing radicals withdifferent activities to 4-anilinoquinazoline derivatives to prepare a series of novel 5,6,7-trialkoxy-N-aryl-substituted-4-aminoquinazoline compounds. The compound has good inhibition on protein phosphorylation, good application prospects in medicines for preventing and treating malignant tumor, and a drawing of the abstract is one of results of tests for influence of the compounds on the proteinphosphorylation of prostatic cancer cells PC3.
CN103462936A Tablet capsule filled with topiramate tablets The invention relates to an oral hard capsule, and in particular relates to a tablet capsule filled with topiramate tablets with different specifications. The tablet capsule filled with the topiramate tablets provided by the invention comprises a capsule and tablets in the capsule, wherein the capsule comprises an upper capsule body and a lower capsule body; 2-3 tablets with the topiramate as the active ingredient are filled in the capsule; one of the topiramate tablets is of an immediate release type; and the rest of topiramate tablets are of controlled release type. The invention has the following beneficial effects that the capsule filled with the topiramate tablets with different specifications is provided; as the content tablets are different in specification and quantity, the medication requirements for different doses can be met; and as the immediate release type tablet and the controlled release type tablets are combined, the trouble of patient in taking medicine is reduced, the in-vivo concentration of the medicine is stable, the medicine within an effective concentration range is slowly released, the patient compliance is improved, and the curative effect on a disease is improved.
EP1021402B1 Aromatic c16-c20-substituted tetrahydro prostaglandins useful as fp agonists The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, X, Y, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of said formula, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.
CN103099775A Adapalene gel The invention provides an adapalene gel. The adapalene gel comprises adapalene serving as an active ingredient, water, humectant, surface active agent, carbopol and neutralizer, wherein the water, humectant, surface active agent, polyacrylic acid and neutralizer are adopted as the auxiliary materials; and the adapalene gel is characterized by comprising sodium calcium edetate.
WO2008012534A2 Retinoids and small molecules as nrf2 antagonists for use in the treatment of diseases associated with abnormal cell proliferation The present invention relates to an improved assay for identifying compounds that may be of use in conjunction with cancer chemotherapeutic agents and anti-proliferative agents, to improve efficacy of such agents and/or render effective compounds with relatively little therapeutic activity. There is also provided a class of compounds of formula (I) and retinoids identified by said assay which may be used in a combination therapy, with current and novel agents, to treat cancers and other diseases associated with abnormal host cell proliferation, such as psoriasis.
US20100178259 Reducing fibrosis using matrix metalloproteinase inhibitors Methods and compositions to prevent scarring of the skin include a matrix metalloproteinase inhibitor and a vehicle suitable for topical application. Scarring and damage to the epidermis and extracellular matrix may be reduced and/or prevented. Following skin damage, application of the matrix metalloproteinase inhibitor reduces expansion of the extracellular matrix portion of the skin compared to untreated skin.
US20110021525 P70S6 Kinase Modulators and Method of Use The invention provides compounds and methods for inhibition of kinases, more specifically p70S6 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
WO2014092514A1 Novel compound, pharmaceutically acceptable salt or optical isomer thereof, method for preparing same, and pharmaceutical composition for prevention or treatment of viral diseases containing same as active ingredient The present invention relates to a novel compound, to a pharmaceutically acceptable salt or optical isomer thereof, to a method for preparing same, and to a pharmaceutical composition for the prevention or treatment of viral diseases containing same as an active ingredient. The novel compound according to the present invention not only has low cytotoxicity but also has excellent antiviral activity against picornavirus such as coxsackievirus, enterovirus, echovirus, poliovirus and rhinovirus, and thus can be effectively used as a pharmaceutical composition for the prevention or treatment of viral diseases such as infantile paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myitis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinus infection, or otitis media.
US20100215633 Method for feeding dairy cows and dairy goats supplements to increase the C2 hxroylated estrogen (C2) to C16 hydroxlated estrogen (C16) ratio secreted in their urine A feed supplement for dairy cows and goats containing various combinations of whole soy, muscadine grapes, Kudzu leaves, brassica group vegetable and or their chemical constituents designed to shift estrogen metabolism towards favorable estrogen chemistry.
US20110039875 Pharamaceutical compositions for treating chronic pain and pain associated with neuropathy The present invention provides methods and compositions for the treatment of neuropathic pain. In certain embodiments, compositions comprising an dextromethorphan (or other N-methyl-D-aspartate receptor antagonist), tramadol, and gabapentin can synergistically act to reduce pain in a human patient. Pharmaceutical compositions may also comprise a capsaicinoid, an esterified capsaicinoid, and/or a tricyclic antidepressant.
US20070264194 Peptides That Bind To Atherosclerotic Lesions The present invention provides peptides that selectively bind to mammalian atherosclerotic lesions. The present invention also provides methods for in vivo identification of peptides capable of binding to biomolecules as well as methods for identifying the targets of such binding moieties. Methods to diagnose or treat pathologic conditions that involve atherosclerotic lesions are also provided by the invention that involve administering to a mammal a peptide attached to a reporter molecule or a therapeutic agent, respectively.
CN102203061A Selective seprase inhibitors Novel radiopharmaceuticals that are useful in diagnostic imaging and therapeutic treatment of disease characterized by overexpression of seprase include complexes that contains a proline moiety and a radionuclide adapted for radioimaging and/or radiotherapy (Formulae I & II).
US20110224178 Composition and method for treating erectile dysfunction Erectile dysfunction in a male human patient is ameliorated by oral administration to the patient of a phosphodiesterase type 5 (PDE5) inhibitor, such as sildenafil, and a glucocorticoid such as prednisone.
WO2008034621A2 Nucleotide phosphorylase for the prophylaxis, treatment or diagnosis of acute lung injury (ali) The invention relates to a medicament for the prophylaxis and/or treatment, or diagnosis of acute lung injury (ALI), to methods for diagnosing a predisposition to ALI or for diagnosing the disease in a living being and to a pharmaceutical or diagnostic composition.
CN101797220A Oxaliplatin chitosan-stearic acid grafting micelle and application The invention provides an oxaliplatin chitosan-stearic acid grafting micelle which comprises 0.5 percent of chitosan-stearic acid grafting, 0.009-0.02 percent of oxaliplatin, 0-0.2 percent of lecithin and the balance of water. The oxaliplatin chitosan-stearic acid grafting micelle is respectively prepared by using a probe ultrasonic method, a film dispersion method and a lecithin mediated film dispersion method. The oxaliplatin chitosan-stearic acid grafting micelle has rapid ingestion function of passive targeting and cancer cells in a polymer micelle, can greatly improve the intracellular medicine concentration of a molecular target in the oxaliplatin in the cancer cells by encapsulating the oxaliplatin chitosan-stearic acid grafting micelle on the oxaliplatin, improves the cytotoxicity and shifts the multidrug resistance, and enhances the clinical anti-tumor efficacy of the oxaliplatin. The oxaliplatin chitosan-stearic acid grafting micelle can be applied to preparing an anti-tumor medicine.
CN102180780A Indenone derivative and applications thereof as developing agent and aggregation inhibitor of amyloid protein deposit and neurofibrillary tangle The invention relates to a compound in a general formula (1), applications of pharmaceutically acceptable salt, esters, amides or predrug of the compound as a developing agent and an aggregation inhibitor of amyloid protein deposit and neurofibrillary tangle, a preparation method of a labeled compound used for development, and a method for conveying the compound to the amyloid protein deposit and the neurofibrillary tangle. When the compound is taken as the developing agent used for detecting in vivo or tissue amyloid protein deposit and neurofibrillary tangle, appropriate radioactive isotope or a contrast agent applicable to magnetic resonance detection needs to be used for labeling the compound. The compound is especially used for the diagnosis and treatment of patients with amyloid protein deposit and neurofibrillary tangle diseases including Alzheimer disease.
EP1670448B1 Hcv inhibiting sulfonamides The present invention concerns sulfonamide derivatives having the general formula (I) and N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs and esters thereof, wherein Q1 is -S- or -O-; R1 is hydrogen, C1-6alkyl, hydroxy, amino, halogen, aminoC1-4alkyl and mono-or di(C1-4 alkyl)amino; R2 is hydrogen or C1-6 alkyl; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4 alkyl, or arylC1-4 alkyl; R4 is hydrogen, C1-4 alkyloxycarbonyl, carboxyl, optionally mono- or disubstituted aminocarbonyl, mono- or di(C C1-4alkyl)aminocarbonyl, C3-7cycloalkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6alkyl optionally substituted with one or more substituents each independently selected from aryl, Het<1>, Het<2>, C3-7cycloalkyl, C1-4alkyloxy-carbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4 alkyl)aminocarbonyl, aminosulfonyl, C1-4alkylS(=O)t, hydroxy, cyano, halogen or amino optionally mono- or di-substituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-4 alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, Het<1>, Het<2> Het<1>C1-4alkyl and Het<2>C1-4 alkyl; Q2 is a radical of formulae (III, IV, V, VI, VII) for the manufacture of a medicament useful for inhibiting HCV activity in a mammal infected with HCV. The present invention also relates to the use of said sulfonamides in pharmaceutical compositions aimed to treat or combat combined HCV and HIV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present sulfonamides with other anti-HCV agents and/or anti-HIV agents.
WO2014011120A1 Endoperoxides, synthesis and uses thereof for the treatment of neoplastic diseases such as cancer The present invention generally relates to processes and methods for the synthesis of endoperoxide compounds. More specifically, the invention relates to a method for preparing endoperoxide compounds starting from an aryl imine of formula (I) in the presence of a metallic catalyst and oxygen. The present invention also relates to endoperoxide compounds of formula (III) and their pharmaceutically acceptable salts thereof, useful for therapy. All substituents are defined herein. Also disclosed are methods of treating cancer using the compounds of formula (III).
US20110190334 Heterocyclic Sulfonamide Derivatives The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.
CA2278694C Sulfamide-metalloprotease inhibitors This invention relates to sulfamides of formula (I) wherein R1, R2, R3, R10, R20, R21 are as defined in the specifications and the claims that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
CN102532082A 2,2-dimethyl benzopyran compound and preparation method and application thereof The invention discloses a 2,2-dimethyl benzopyran compound and a preparation method and application thereof, belonging to the technical field of medicines. The structure of the 2,2-dimethyl benzopyran compound is shown in a figure described in the specification. The preparation method of the 2,2-dimethyl benzopyran compound comprises the following steps of: with 2-methyl-butyl-3-alkyne-2 alcohol as a starting raw material, carrying out four-step reactions comprising chlorination, Williamson etherification, cyclization and Aldol condensation to obtain the 2,2-dimethyl benzopyran compound. The preparation method of the 2,2-dimethyl benzopyran compound, disclosed by the invention, has the advantages of simple operation, convenience for post-treatment and higher yield. The 2,2-dimethyl benzopyran compound has an excellent inhibition function on various cancer cells so as to be applied to treatment of tumors. A formula is described in the specification, wherein R' represents H and C1-6 alkyl and R represents substituted or unsubstituted aromatic ring or heteroaromatic ring.
US20080081825 5-((2,4-difluorophenyl) {[(1-methyl-4-piperidinyl)oxy]imino}methyl)-1-(2,6-dimethylphenyl)-2(1H)-pyridinone; p38 MAP kinase and tumor necrosis factor inhibitor; inflammatory cytokines or chemokine, respiratory diseases, cardiovascular diseases and bone diseases The present invention provides a compound having p38 MAP kinase inhibitory activity. Because of having p38 MAP kinase inhibitory activity, the compounds represented by the formula (I): wherein each symbol is as defined in the description, salts thereof, N-oxides thereof, solvates thereof, or prodrugs thereof are useful in preventing and/or treating diseases that are supposedly caused or deteriorated by abnormal production of cytokines including inflammatory cytokines or chemokines, or by overresponse thereto, namely cytokine-mediated diseases such as inflammatory diseases, respiratory diseases, cardiovascular diseases and bone diseases.
CN101687900A Double-stranded locked nucleic acid compositions Immunostimulatory agents, including nucleic acids having one or more than one locked nucleic acid (LNA) nucleosides are provided. The nucleic acids may further comprise CpG motifs. The nucleic acids may be double stranded, and may comprise dsRNA.
CN1723909A Soft capsule contg. arasaponin (Panax Pseudoginseng leaves glucoside), and its prepn. method An arasaponin soft-capsule is composed of the liquid medicine prepared proportionally from arasoponin, diluent and surfactant, and the shell prepared from gelatin, glycerin, water, anti-oxidizing agent and antiseptic. Its preparing method is also disclosed.
WO2006122183A3 Injectable hydrogels and methods of making and using same A biocompatible hydrogel and method for augmenting soft and hard tissue, wherein the hydrogel comprises at least one gel former and the hydrogel is used to augment tissue when introduced into a desired tissue site. The hydrogel may comprise at least one of a carbomer, a poloxamer and a combination thereof. The hydrogel may have a yield strength of about 300 gm/cm-sec to about 12,000 gm/cm-sec and require less than about 10 lbf to extrude the hydrogel from a 1 cc syringe having a 25 gauge 1/2' length needle at a rate of 2 inches per minute.
CN102442997A Quinoline derivative as well as preparation method thereof, midbody and application thereof The invention discloses a quinoline derivative shown as a formula A as well as a preparation method thereof, a midbody and an application thereof, wherein X is O, S or N(CH3), R1 is OCH3 or halogen, R2 is H or F, and R is H or halogen or alkyl or alkoxy. The quinoline derivative has good activity for inhibiting HMG-CoA reductase and can be used for preparing medicine for inhibiting the HMG-CoA reductase or treating hyperlipidemia relevant diseases.
CN101797385A Oral calcium pharmaceutical composition The invention relates to an oral calcium pharmaceutical composition, which is a preparation prepared by taking calcium salt, vitamin D, boron compounds, copper compounds, magnesium compounds, manganese compounds, zinc compounds and at least one transfer substance capable of promoting calcium and mineral matter absorption of human body as active ingredients, and mixing with pharmaceutically-accepted auxiliary materials or subsidiary components. The oral calcium pharmaceutical composition can effectively supplement various trace elements necessary for human body such as calcium, copper, zinc, magnesium, manganese, boron and the like at the same time, and is used for preventing or curing diseases like osteoporosis.
US7709460 co-administration of a glutathione precursor (N-acetyl cysteine or alpha -lipoic acid) and hydroxocobalamin (a derivative of Vitamin B12) to patients with a functional Vitamin B12 deficiency and suffering from a neuropsychiatric abnormality A method and medical composition for the treatment and/or prevention of a functional Vitamin B12 deficiency in an individual that is brought about as a consequence of oxidative stress on biochemical pathways. The functional Vitamin B12 deficiency may eventually present as dementia, other neuropsychiatric abnormality and/or vascular disease. The method involves the administration of a medical composition that supplies a cobalt-sulphur bond in the upper β-ligand of an intracellular cobalamin molecule thereby facilitating intracellular processing of cobalamin. The cobalt-sulphur bond may be provided directly by administration of a thiolatocobalamin, such as glutathionyl-cobalamin or indirectly by the co-administration of Vitamin B12 (or a derivative thereof) with a sulphur-containing molecule, such as glutathione or a precursor thereof.
US20120083443 Control of ATP Release by Red Blood Cells and Therapeutic Applications Thereof The invention is based upon the discovery that red blood cells contain phosphodiesterase 3B (PDE3B), and that inhibition of that phosphodiesterase allows for an enhanced accumulation of cAMP and subsequent release of ATP. It was further discovered that RBCS treated with insulin accumulate significantly less cAMP and release significantly less ATP than normal RBCS. Likewise, RBCS of patients suffering from type 2 diabetes (hyperinsulinemia) accumulate significantly less cAMP and release significantly less ATP than normal RBCS. It was further discovered that prostaglandin analogues synergistically work with phosphodiesterase 3B inhibitors to improve or increase cAMP accumulation and ATP release RBCS. Thus the invention is directed to compositions and methods for improving ATP release by RBCS, via administering PDE3B inhibitor or a combination of PDE3B inhibitor and prostaglandin analogue.
CN1907293B Combined medicine for treating lpneumonia and preparing process thereof The invention discloses a pneumococcus combined agent and preparing method, which comprises the following parts: 40-500g Azithromycin/potassium dehydroandrographolide succinate at random weight proportion, 20-40g reduced glutathione and vitamin E at 1: 2-3; 100-200g hydroxypropyl-beta-cyclodextrin, 100-200g vitamin C and glycine at 2-4:1.
US20090205062 Caspase-9 deficient animals and the use thereof The invention relates to genetically manipulated animals that are deficient in the expression of Casapse-9, a protein involved in programmed cell death. The invention further relates to methods for preventing specific types of cell death associated with Caspase-9 activation.
US20110027389 Low Viscosity Liquid Polymeric Delivery System Low viscosity biodegradable polymer solutions of a liquid biodegradable polymer and biocompatible solvent and methods of using the compositions to form a biodegradable liquid polymer implant are provided.
CN103255187A Low molecular hyaluronate, preparation method and purpose thereof The invention belongs to the fields of enzymology and pharmaceutical chemistry, and relates to the low molecular hyaluronate, preparation method and purpose thereof. Concretely, the preparation method comprises a degradation step of hyaluronic acid or salt thereof whose molecular weight is greater than 1000 kDa by hyaluronidase prepared by Bacillus spp whose preservation number is CGMCC No. 5744 or SEQ ID No:2 coded hyaluronidase. The preparation of low molecular hyaluronic acid or salts thereof by using hyaluronidase produced by Bacillus spp of the present invention has the advantages of simple operation, mild condition, non-destroy of the product structure and low cost. The product is suitable for large scale industrialized production. The low molecular hyaluronate prepared by the invention has the advantages of good transdermal absorbency, good purity, non-cytotoxicity, good antioxidation, etc., and can be used in the fields of cosmetic, foodstuff and medicine.
US20130065886 Administration of benzodiazepine compositions The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.
CN103550303A Pharmaceutical composition for preventing and treating canine otitis externa The invention discloses a pharmaceutical composition for preventing and treating canine otitis externa, and belongs to the field of a veterinary medicine. The pharmaceutical composition consists of the following components: 2.0-3.0g of florfenicol, 0.2-0.4g of metronidazole, 0.5-3.0g of clove extract and 0.5-3.0ml of tea tree oil in per 100ml of a solution, wherein propylene glycol is taken as a solvent. Furthermore, the invention discloses a preparation method and application of the pharmaceutical composition. The pharmaceutical composition has high curative effect on canine otitis externa; in addition, the pharmaceutical composition, which contains natural extract that is complex in components, can reduce possibility of drug tolerance of bacteria, keep efficacy for a long period and facilitate accurate administration; furthermore, the pharmaceutical composition disclosed by the invention is high in efficacy, and can reduce duration and times in treating canine otitis externa, relieve pain in animals and enhance animal welfare.
CN102327254A Application of ethanol as ionizing radiation protectant The invention belongs to the field of radiation protective reagents, and particularly relates to new application of ethanol as a radiation protective reagent. In the application, before radiation, breast cancer macrophage chemotactic factor-7 (MCF-7) cells are treated for 2 hours by 50 to 100mM ethanol, and after 6Gy of x-rays irradiate, gap phase/mitotic phase (G2/M) arrest, a sub-G1 peak and apoptotic ratios of early and later periods of the radiated breast cancer cells can be reduced, and the injury effect of radiation on the breast cancer cells can be relieved, so the formation of irradiated cell cloning is increased effectively. Compared with a simple irradiation group, an irradiation group with combined 100mM ethanol and 6Gy of x-rays has the advantages that the forms of the MCF-7 cells are integral, and the cell state is better. Furthermore, 100mM ethanol has a certain protective effect on injury caused by 6Gy of x-rays, and the radiation resistance of the MCF-7 cells can be increased.
CA2514552C Adjuvant used in dielectric heating-assisted cancer treatment, and cancer treatment method There is provided an adjuvant capable of enlarging an ablation area and reducing ablation unevenness in a dielectric heating-assisted cancer treatment such as radiofrequency ablation used for treatment of hepatic cancer. The adjuvant includes a conductive substance such as a metal element (e. g.,iron) and a pharmaceutically acceptable carrier of lipid dispersion, polymer solution or polymer dispersion.
EP1607090A1 Asimadoline for the treatment of irritable bowel syndrome Production of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidino) ethyl]-2,2-diphenylacetamide (Ia) or N-methyl-N-[(1R)-1-phenyl-2-((3R )-3-hydroxypyrrolidino)ethyl]-2,2-diphenylacetamide (Ib) comprises (a) reacting the corresponding enantiomer of an N-substituted phenylglycine derivative with an optionally O-protected 3-hydroxypyrrolidine derivative, (b) reducing the product to convert the N-substituent to methyl and remove any protecting group, and (c) reacting with an activated diphenylacetic acid derivative. Production of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidino) ethyl]-2,2-diphenylacetamide (Ia) or N-methyl-N-[(1R)-1-phenyl-2-((3R )-3-hydroxypyrrolidino)ethyl]-2,2-diphenylacetamide (Ib) comprises (a) reacting the corresponding enantiomer of an N-substituted phenylglycine derivative of formula (II) with an optionally O-protected 3-hydroxypyrrolidine derivative of formula (III), (b) reducing the product of formula (IV), and (c) reacting the product of formula (V) with an activated diphenylacetic acid derivative of formula (VI) to give a product of formula (Ia/Ib): [Image] [Image] [Image] [Image] R : H, OR1> or SR1>; R1>A, aryl, heteroaryl, Si(R3>)3 or COR3>; R3>H, A, aryl or heteroaryl; A : 1-6C alkyl; M : H, alkali(ne earth) metal, NH4 or alkylammonium; R2>H, A, aryl, heteroaryl, Si(R3>)3 or COR3>; R4>halogen, OA or OCOA. An independent claim is also included for compounds referred to as N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidino)ethane] and N-methyl-N-[(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidino)ethane] useful as intermediates for (Ia) and (Ib). - ACTIVITY : Antiinflammatory; analgesic; diuretic. - MECHANISM OF ACTION : None given.
CN101023993A Chloasma diminishing medicine containing deer foetus and functional food and preparing method The present invention relates to a product containing deer's fetus, said product can be used as medicine, also can be used as functional food for removing chloasma and its preparation method. Said product is made up by using (by weight portion) 20-200 portions of deer's fetus, 30-150 portions of Chinese angelica root or its extract, 40-120 portions of pilose asiabell root or its extract, 40-200 portions of white peony root or its extract and 2-20 portions of vitamin E. Said product can be made into tablet preparation and capsule preparation.
WO2005000285A3 METHODS OF TREATING NON-INFLAMMATORY GASTROINTESTINAL TRACT DISORDERS USING Cav2.2 SUBUNIT CALCIUM CHANNEL MODULATORS A method is provided for using Cav2.2 subunit calcium channel modulators to treat non-inflammatory gastrointestinal tract disorders.
US20060177420 treatment of a tumor by administering to a patient an effective amount of active dendritic cells (DC) that are tumor-specific and secrete IL12 The present invention discloses the use of active dendritic cells (DCs) releasing interleukin 12 (IL-12) which are loaded with an antigen against a specific pathogen or a specific tumor and, due to the treatment with lipopolysaccharide (LPS) and interferon-gamma (IFN-γ), release IL-12, for the preparation of a medicament for treating a patient having an infection with said specific pathogen or for treating a patient having said specific tumor.
US20090069429 Compositions Comprising Alpha-Ketoglutarate and Their Use for Modulating Muscle Performance This invention relates to a composition comprising Alpha-ketoglutarate (AKG) for modulating muscle performance in a mammal including a human being. Also contemplated is a method for modulating muscle performance in a vertebrate, including mammal and bird, and the manufacture of a composition for the prevention, alleviation or treatment of muscle performance in said vertebrate.
CA2275060C Novel triglyceride and composition comprising the same The present invention provides a novel triglyceride and a composition containing that novel triglyceride having a triglyceride structure of the human breast milk type, which triglyceride has a saturated fatty acid having 16-18 carbon atoms at the position 2, at the position 1 and/or 3; which is and at least one .omega.6, .omega.9 or .omega.3 unsaturated fatty acid manufactured by subjecting a glyceride in which a saturated fatty acid having 16 to 18 carbon atoms is bonded at position 2 to transesterification using a lipase and a .omega.6, .omega.9 or .omega.3- unsaturated fatty acid.
CN101932313A Use of hedgehog agonists in the treatment of musculoskeletal-related disorders The invention provides methods for the diagnosis and treatment of musculoskeletal disorders relating to the Hedgehog pathway, including but not limited to muscular dystrophy (e.g., Duchenne Muscular Dystrophy) using agents that agonize Sonic Hedgehog (shh), and thereby, the Hedgehog signaling pathway. Said agonizing agents include, e.g., the compounds of the invention (e.g., a compound of Formula I). The invention also provides methods of screening for agents that are capable of increases the proliferation of muscle and/or muscle precursor cells.
CN101194902A Dropping pills containing ubenimex and method for preparing the same The invention provides a medicament which can enhance immune function. The invention overcomes the shortcomings of the prior dripping pills that pure natural degrees of findings which are used by the prior dripping pills are not high, and chemosynthesis findings which are commonly used are not in food additives catalogs of some countries, and tastes of the dripping pills are worse. The invention is a pharmaceutical preparation whose natural degree is higher, safety is stronger, and side effect is lower.
US20090209540 Novel Biaryl Benzolmidazole Derivatives and Pharmaceutical Composition Comprising The Same Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.
CN103360379A Novel oxazolidinone compound The invention provides a novel and effective oxazolidinone derivative, as well as an isomer, a pharmaceutically acceptable salt, a chemical protection form and a prodrug thereof.
CN101205193A Salt compound formed by aceclofenac and organic base as well as composition and uses thereof The invention discloses a salt compound formed through the aceclofenac and the organic base and the assemblage and the use. The general formula of the salt compound is AxR mH2O; wherein, A is the aceclofenac (CAS RN: 89796-99-6) and x is 1, 2; R is nitrogen organic base and can be amine and basic amino acid. The amine is most suitable for being selected from the Meglumine and trometamol; the basic amino acid is most suitable for being selected from the Arginine, Lysine, Ornithine, Histidine and Citrulline. The spatial configurations of the amino acids include the DL type, D type, L type and optimized L type; m is 0, 1, 2, 3, 4, 5 and 6. The compound and the assemblage to which the invention relates can be applied to the diseases such as the inflammation and pain, sprain, pull, and other soft tissue injuries and fever, etc., caused by the rheumatoid arthritis, rheumatoid arthritis, osteoarthritis, spondylitis, etc. of the human beings or animals.
WO2009101135A1 Combined use of 25-hydroxy-vitamin d3 and vitamin d3 for improving bone mineral density and for treating osteoporosis We disclose the combined use of vitamin D (cholecalciferol) and 25-OH D3 (calcifediol) to treat and/or prevent osteoporosis. One or more bisphosphonate compounds to inhibit bone resorption may also be used. Forms and dosages of a pharmaceutical composition, as well as processes for manufacturing medicaments, are also disclosed.
WO2014142660A1 Combinations of inhibitors of mek, egfr and erbb2 in the treatment of kras-mutant lung cancer and kras-mutant colon cancer The current disclosure relates to pharmaceutical combinations and compositions useful in the treatment of certain types of cancer. The disclosure also relates to method of treatment these certain types of cancer. In particular, the disclosure relates to the combined use of inhibitors of MEK, EGFR and ERBB2 in the treatment of KRAS-mutant lung cancer, and KRAS-mutant colon cancer.
EP2684456A1 Fungicidal and bactericidal composition that comprises volatile organic compounds of natural origin The present invention relates to a composition with fungicidal and bactericidal activity, which comprises volatile organic compounds (VOCs) obtained from plants and microorganisms, in which said VOCs are C4-C12 fatty alcohols or cyclic alcohols or phenol-derived compounds, or terpene-derived compounds, and also derivatives and mixtures thereof. Furthermore, the present invention likewise relates to the use of said compositions in the protection of agricultural crops, in post-harvest treatments, in food preservation and in the disinfection of facilities and equipment.
CN101185633A Neratinib sustained-release implant for treating solid tumor A sustained release implant includes 0.1%-50% (w/w) nilotinib, 50-99% sustained release excipients and 0-15% sustained release moderator. Sustained release excipients are mainly one or combination of poly (L-lactide-co-ethyl phosphate), poly (L-lactide-co- phosphoric acid propyl), polylactic acid, the copolymer of polylactic acid and hydroxyacetic acid and polifeprosan; sustained release moderator is one or combination of mannitol, sorbic alcohol and chondroitin; sustained release implant applied in local tumor can slowly release nilotinib onto local tumor, thus maintaining effective drug concentration of local tumor as well as significantly reducing overall toxic reaction; the invention not only reduces overall toxic reaction of nilotinib, but also selectively improves drug concentration in local tumor, enhancing the therapeutic effects of non-operative therapy such as chemotherapy drugs and radiotherapy. The implant can be used for treating solid tumors including lung cancer, esophageal carcinoma, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic carcinoma, pancreatic cancer, bladder carcinoma, cerebroma, and colorectal cancer.
US7381718 new process for the preparation of a key intermediate A process for the preparation of compounds of formula (I) in which R1, R2, R3 and n are defined as indicated in the description, use of said compounds as intermediates for the preparation of estrogen derivatives as well as the intermediates of this process.
US20070249695 Preventive and/or Therapeutic Agents for Meniere's Disease The present invention relates to preventive and/or therapeutic agents for Meniere's disease, which comprise a leukotriene antagonist (such as pranlukast hydrate) as an active ingredient. Leukotriene antagonists (such as pranlukast hydrate) are effective in ameliorating various symptoms, such as hearing impairment, tinnitus, a feeling of fullness in the ear and vertigo, thus being useful as a preventive and/or therapeutic agent for Meniere's disease.
CN103285365A Drug for preventing chilblain and preparation method thereof The invention belongs to the technical field of pharmaceutical chemicals, and particularly relates to a drug for preventing chilblain. The drug is characterized by comprising the following materials in parts by weight: 4-8 parts of deionized water, 1-3 parts of sheep horn powder or ox horn powder or antler powder of which the fineness is smaller than 150 meshes, 7-9 parts of flowers carthami, 2-4 parts of mint, 4-8 parts of rhizoma zingiberis, 1-3 parts of ginseng, 3-5 parts of pseudo-ginseng, 4-6 parts of borneol, 60-80 parts of vaseline, 12-18 parts of glycerol, 2-4 parts of urea, 0.4-0.6 parts of methylhydroquinone, and 2-5 parts of hydroxyethyl carbon amide. The invention also discloses a preparation method of the drug for preventing chilblain. The drug has the following beneficial effects that preparation is simple, quality guarantee period is long and prevention effect is good, so that the skin is elastic, bright, and the like. The drug has fragrance, and is more comfortable when a user uses the drug.
CN102397412A Foot bath liquid for treating tinea pedis The invention discloses foot bath liquid for treating tinea pedis and relates to the technical field of bath supplies. A preparation method comprises the following steps of: mixing 4 percent of phellodendron, 4 percent of sophora flavescens, 3 percent of atractylodes lancea, 3 percent of plantain, 4 percent of Chinese honeylocust fruit, 4 percent of pepper, 3 percent of portulaca oleracea, 5 percent of alum and millet wine in a formula and soaking for twice, and continuously decocting medicinal residuals; mixing medicinal liquor which is obtained by two times of soaking, and mixing uniformly, and concentrating mixed medicinal liquid to form paste; adding water into medicinal residuals and decocting for three times, and discarding the medicinal residues; and mixing decoction which is obtained through three times of decoction, mixing uniformly, heating and concentrating to form paste, mixing decoction paste and soak solution paste uniformly, adding 20 percent of deep sea mineral salt, 5 percent of deep sea seaweed, and 3 percent of safflower, mixing uniformly, bottling and sealing. The foot bath liquid has the cleaning, health-care, bacteriostatic and bactericidal effects, is convenient to use, can effectively remove old cutin on the surface layer, ensures that the medicinal effect is quickly exerted through skin, reaches main and collateral channels of a whole body, invigorates the blood circulation and relaxes tendons, and can effectively treat tinea pedis, dermatophytosis, and foot pruritus.
US20100267835 Methods of treating disorders of trigeminalvascular activation Alpha-aminoamide derivatives useful in the treatment of disorders of trigeminalvascular activation are disclosed.
WO2012007729A3 Pharmaceutical compositions comprising r (+) budesonide and one or more bronchodilators A pharmaceutical composition for inhalation comprising R (+) budesonide and one bronchodilators, and, optionally, one or more pharmaceutically acceptable excipients.
CN102898284A 3-allyl-[1,1'-biphenyl]-4-phenol, derivatives, preparation methods and uses thereof The present invention belongs to the field of chemical medicine, and particularly relates to 3-allyl-[1,1'-biphenyl]-4-phenol, derivatives, preparation methods and uses thereof. A technical problem solved by the present invention is to provide a new class of compounds: 3-allyl-[1,1'-biphenyl]-4-phenol represented by a formula I and derivatives thereof. Experiment results of the present invention show that 3-allyl-[1,1'-biphenyl]-4-phenol represented by the formula I and the derivatives thereof have good effects of anti-tumor, anti-angiogenesis, anti-oxidation and other disease resistance, and provide a new selection for drug preparation.
CA2206362C Substituted 1-naphthoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them Substituted 1-naphthoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them. Substituted 1-naphthoylguanidines of the formula I see formula I in which R2 to R8 have the meanings indicated in the claims, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. They also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the production of ischemically induced cardiac arrhythmias.
CN101305005A Novel diazaspiroalkanes and their use for treatment of CCR8 mediated diseases The invention provides compounds of general formula (I) wherein A, B, p, w, x, y, and z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
US20100298445 Optimized Fluorocarbon Emulsions for Blood Substitutes and Other Therapeutic Uses The present invention is directed to a stable fluorocarbon emulsion having a continuous aqueous phase and discontinuous fluorocarbon phase comprising two fluorocarbons and surprisingly demonstrates that perfluorodecyl bromide is as effective in stabilizing perfluorooctyl bromide emulsions of certain concentrations than much more highly concentrated perfluorooctyl bromide/perfluorodecyl bromide emulsions without the significant problems experienced in higher concentrated emulsions such as longer organ retention times, formation of PFDB crystals, larger emulsion particles, manufacturing problems and inability of repeat dosing inherent with higher concentrations of perfluorodecyl bromide.
US20100143475 Transdermal therapeutic system with two-phase release profile The present invention relates to a transdermal therapeutic system (TTS) consisting of an impermeable coating, a matrix containing an ergoline compound having the formula (I) or a physiologically compatible salt or derivative thereof, wherein R1 denotes an H atom or a halogen atom and R2 is an alkyl group having 1 to 4 carbon atoms and
WO2013017807A1 Antiseptic composition The invention relates to an antiseptic composition. The composition comprises an association of at least silver metal, preferably in a micronised form, and hyaluronic acid or one of the salts thereof having a molecular weight of between 50 kDa and 2000 kDa. The invention can be especially applied to the field of veterinary medicine, for the treatment of skin wounds and the healing thereof.
CN1887352A Composition for treating eye's fungal and bacterial infection The present invention discloses one kind of composition for treating eye's fungal and bacterrial infection. The composition has at least one of mercury preservatives, including merthiolate, merphenyl nitrate, merphenyl nitrate alkali, phenylmercuric acetate, phenylmercuric borate, etc as well as their salts and derivatives as the main active component; supplementary material including antioxidant, pH regulator and osmotic pressure regulator; and water as the solvent and carrier. The composition may be prepared into different preparation forms for treating eye's fungal and bacterrial infection.
WO2013061669A1 Benzohydrazide derivative for inducing g2/m phase arrest and cell death The invention pertains to a specific carbazole derivative and pharmaceutical use thereof. The compound provided by the invention provides the following compound that can be utilized as an anticancer drug or anticancer drug seed. In the formula (I), R1-3 are each independently a hydrogen atom, halogen atom, nitro group, hydroxy group, optionally substituted C1-6 alkyl group, optionally substituted C1-6 acyl group, or optionally substituted C1-6 alkoxy group.
WO2014136036A1 Nutritional and medicinal oral composition for veterinary use The invention relates to a nutritional and medicinal oral composition for veterinary use, comprising a core of an extruded product of complete feed coated with at least one layer of fatty material, said layer of fatty material comprising at least one active substance in a microparticulate form selected from benazepril, benazeprilat and a pharmaceutically acceptable salt thereof, said active substance being (i) pre-conditioned in the form of an oily suspension of said active substance or (ii) pre-conditioned in the form of waxy granules of said active substance.
CN102670613A Medicine composition for improving dissolution of indiplon and preparation method of medicine composition The invention relates to a novel composition of indiplon with low dissolvability in a water-based solvent, a method for preparing the novel composition, and an oral preparation comprising the novel composition. More particularly, the invention relates to an oral composition of the indiplon, which has the function of improving the dissolution. The novel composition is characterized by comprising micronized indiplon, wherein micronization technologies comprise fluid energy milling, ball grinding, recrystallizing, solid-state dispersing and the like. A solid composition also comprises at least one solubilizer selected from Tween-80 or lauryl sodium sulfate. The invention also relates to a preparation method of the novel composition and the oral preparation prepared by adopting the preparation method. According to the invention, the composition of indiplon for improving oral absorption through improving dissolution can be obtained. The oral solid composition of indiplon can express that the dissolubility is improved under the in vitro dissolution condition.
CN101932563A Solid forms of (s)-2-amino-3-(4-(2-amino-6-((r)-2,2,2-trifluoro-1-(3'-methoxybiphenyl-4-yl)ethoxy)pyrimidin-4-yl)phenyl)propanoic acid and methods of their use Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-2,2,2-trifluoro-1-(3'-methoxybiphenyl-4-yl)ethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed.
US20120316215 Compositions and methods for treating metabolic disorders Disclosed are methods for treating a subject suffering from phenylketonuria and/or phenylalanemia. The methods include, in part, enterally administering to the subject a LNAA supplement in which the weight ratio of Leu to Val is greater than 2:1; in which the weight ratio of Leu to iLeu is greater than 3:1; or which includes one or more LNAAs and which further includes Lys. LNAA supplements are also disclosed. Also disclosed are methods for treating a subject suffering from a condition involving a metabolic disorder involving the metabolism of a first amino acid X. The method includes enterally administering to the subject a composition which (i) is substantially free from the first amino acid X and (ii) which includes a second amino acid Y that competes with amino acid X at a gastrointestinal tract transporter.
CN102942497A Preparation and application of amino substituted carboxylic acid compounds The invention relates to two novel amino substituted carboxylic acid compounds and a preparation method thereof. The compounds can be used for the prevention and treatment of in-vivo metal poisoning and the preparation of metal decorporation medicaments and health products. The amino substituted carboxylic acid compounds combine the advantages of aminocarboxylic acid and phenolic hydroxyl; and the two novel chelators designed by effectively introducing carboxyl chelation groups onto the benzylic site of a benzene ring have fine metal poisoning prevention and treatment activity and metal decorporation activity. By adding the effective chelation groups on the benzylic site in the molecule chelation center, the nuclide ion bonding capability is enhanced, so that the compounds can be easily formed into stable complexes, thereby accelerating the in-vivo discharge and improving the decorporation effect and poisoning prevention and treatment effect of metal (especially uranium).
WO2012094838A1 Use and pharmaceutical composition of lignosulfonate The present invention discloses the use and pharmaceutical composition of lignosulfonate. Lignosulfonate has strong activity against HIV-1 in vitro. The mechanism is mainly blocking HIV-1 virus from binding to target cells, thereby blocking its infection. Lignosulfonate also has significant inhibitory effect on the CD4 dependent and in-dependent HIV-1 infection. In addition, the result of cell fusion experiments shows that lignosulfonate has the role of inhibiting HIV-1 viral envelope protein-mediated integration. Finally, cytotoxicity experiments show that lignosulfonate has basic non-toxicity to cells in the effective antiviral concentrations. Lignosulfonate has rich source and low production costs. It can be used as a new potential anti-HIV-1 drug and antimicrobial agent.
US20120316140 Analgesic composition and method of making the same A soluble aspirin composition, comprising: (i) granules including aspirin, heat-treated bicarbonate salt, pharmaceutically-acceptable resin and surfactant, in mixture with: (ii) crystalline particles of pharmaceutically-acceptable acid; and (iii) crystalline particles of heat-treated bicarbonate salt; wherein the soluble aspirin composition when introduced to water undergoes reaction of the crystalline particles of pharmaceutically-acceptable acid with the heat-treated bicarbonate salt and the aspirin to effect effervescing action and disintegration of the granules with conversion of the aspirin to an acetylsalicylate compound of the bicarbonate salt cation so that the composition rapidly dissolves in the water without occurrence of undissolved residue. The composition is solublizable within 30 seconds in cool to cold water to provide an effervescent analgesic solution that can be readily orally administered to an individual in need of analgesia.
CN101716348A Construction and application of gold-magnetic nanoparticle-based medicament carrying platform The invention relates to the construction and application of a gold-magnetic nanoparticle-based medicament carrying platform, which belong to the technical field of magnetic nanophase materials. The construction comprises the synthesis of magnetic nanoparticles, the synthesis of an Fe3O4-SiO2 nuclear shell structure, the amine surface modification of the Fe3O4-SiO2 nuclear shell structure, protonation and the electrostatic adherence of gold nanoparticles after the surface modification, the coupling of curcumin and the coupling of mercapto polyethylene glycol PEG-SH so as to prepare a multifunctional gold-magnetic nano-platform. The construction and the application have the following advantages that: the gold-magnetic nanoparticle-based medicament carrying platform is a magnetic carrier with a modified surface and has the characteristics of relatively stronger magnetism, good chemical inertness, biocompatibility, easy functionalization and the like, and can be prepared by a simple method; and the magnetic nanophase materials can be quickly separated with a magnetic field in a suspension system, are highly concentrated and act on tumor cells under the guidance of an external magnetic field, and can be applied in biological fields, such as bioseparation, medicament transportation, biological tags, cell imaging and developing and study on the separation of cells or other biomolecules.
CN103720646A Enriched-Se isatis root polysaccharide oral liquid and preparation method thereof The invention relates to an enriched-Se isatis root polysaccharide oral liquid. Firstly, isatis roots, sodium chloride and water are mixed and heated to extract isatis root polysaccharide, then the collected isatis root polysaccharide and a selenium agent perform a catalytic reaction, and lastly, a reaction product is mixed with sulfactol and the water to obtain the finished product. The enriched-Se isatis root polysaccharide oral liquid has the effects of both the isatis root polysaccharide and organic Se, which are mutually combined and simultaneously act on an organism, can further improve the immunity ability of the organism; in the clinic practical application, the enriched-Se isatis root polysaccharide oral liquid avoids that poultry suddenly die under the state of lacking the Se and abnormal immunity, so as to lower farmers' economical loss.
US20100273866 Diagnosis and treatment of cancer: i A method of diagnosing cancer comprising the steps of (i) obtaining a sample containing nucleic acid and/or protein from the patient; and (ii) determining whether the sample contains a level of SCN5A (and optionally also SCN9A) voltage-gated Na+ channel nucleic acid or protein associated with cancer. A method of diagnosing breast cancer comprising the steps of (i) obtaining a sample containing nucleic acid and/or protein from the patient; and (ii) determining whether the sample contains a level of voltage-gated Na+ channel nucleic acid or protein, preferably SCN5A or SCN9A, associated with cancer. A method of treating cancer comprising the step of administering to the patient an agent which selectively prevents the function of SCN5A (and optionally also SCN9A) voltage-gated Na+ channel. A method of treating breast cancer comprising the step of administering to the patient an agent which selectively prevents the function of a voltage-gated Na+ channel, preferably SCN5A or SCN9A. Genetic constructs and molecules useful in such methods. The methods and compositions are particularly suited to breast cancer.
CA2310950C An efficacious dosage regiment of galantamine that reduces side effects Galantamine has be used in the treatment of a number of chronic diseases. The use of this drug is associated with side effects such as, nausea or vomiting, and headaches.It has been demonstrated that by slowly introducing the patient to the drug these side effects can be reduced. It has also been shown that this slower titration results in the ability to use a lower effective dose of the drug.
US20080254072 Method For Inhibiting Scavenger Receptor-A and Increasing Immune Response to Antigens Provided is a method for enhancing an immune response to a desired antigen in an individual. The method is performed by administering to the individual an agent capable of inhibiting class A macrophage scavenger receptor (SR-A) and optionally administering the desired antigen. Also provided is a method for enhancing an immune response to an antigen by administering to an individual a composition containing antigen presenting cells that are characterized by specifically inhibited SR-A. Substantially purified populations of mammalian dendritic cells characterized by specifically inhibited SR-A are also provided.
CN101912371A Coenzyme Q10-containing injection composition and preparation method thereof The invention relates to a coenzyme Q10-containing injection composition which is characterized by comprising a main functional raw material of reduced type coenzyme Q10, and besides the reduced type coenzyme Q10 as the main functional raw material , the composition also comprises an emulsifier, an assistant, a surfactant and a solvent; wherein the emulsifier is polyethylene glycol or glycerol or the mixture of the polyethylene glycol and the glycerol; the assistant is a plurality of vitamins and amino acid which are required by the human body, or the mixture of the vitamins and a plurality of amino acids; the surfactant is Twain-20 or hydroxypropyl methyl cellulose; the solvent is normal saline or deionized water; and the injection composition is prepared according to the following content in percentage: 3.0-30 percent of the reduce type coenzyme Q10, 0-20 percent of the emulsifier, 0-15 percent of the assistant, 0-10 percent of the surfactant and the balance of the solvent.
WO2011147772A1 Ccr2 receptor antagonists The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
CN101497593A 5-hydroxy coumarin and pyranoid type coumarin compounds, synthesizing method and use The invention relates to a compound of 5-hydroxycoumarin and pyranocoumarin and synthesis and application thereof. The compound has a structural formula I or II; during preparation, according to the mol portion, under the catalytic action of 2 to 6 portions of SO2-OSO3H(silicon sulfonic acid), 1 to 3 portions of 5-iodine-1 and 3-dihydroxyhenzene and 1 to 3 portions of RCOCH2COOCH2CH3 are condensed to obtain the compound of which the structural formula is iodo-5-hydroxycoumarin; 1 to 4 portions of compound of iodo-5-hydroxycoumarin and 2 to 8 portions of 3-methyl-2-crotonaldehyde or 3-chloro-3-methylbutyne are reacted to generate a compound of iodo-pyranocoumarin; and finally, by coupled reaction, the coumarin compound with the structural formula I or II is generated. The IC50 value of the compound on breast cancer cells MCF-7 reaches 3.3 to 18.3, so that the compound can strongly inhibit the breast cancer cells MCF-7.
US20120263779 Biodegradable drug delivery system A drug delivery system (DDS) comprised of segmented biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The segmented implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 50 days and one year, or longer, and permit the DDS to have segments that possess individual and different drug release characteristics.
WO2012096458A2 Process for preparation of phenyl carbamate derivatives Provided are a process for the preparation of phenyl carbamate derivatives, useful in the treatment of CNS (central nervous system) disorders, an intermediate in the synthesis of the phenyl carbamate derivatives, and a process for preparation of the intermediate.
EP1248597B1 Pharmaceutical aerosol formulation of salmeterol and fluticasone propionate There is provided according to the invention a pharmaceutical aerosol formulation which comprises: (i) salmeterol or a phamraceutically acceptable salt thereof, (ii) fluticasone propionate and (iii) a hydrofluoroalkane (HFA) propellant, characterised in that the salmeterol or pharmaceutically acceptable salt thereof and fluticasone propionate are completely dissolved in the formulation.
CN103393592A Sodium azulene sulfonate gel and its preparation method and use The invention discloses sodium azulene sulfonate gel. The sodium azulene sulfonate gel is prepared from 0.05-1 weight part of sodium azulene sulfonate, 0.5-50 weight parts of a gel base material, 1-50 weight parts of a transdermal enhancer, 0.5-2.5 weight parts of a pH conditioning agent, 0.1-0.5 weight parts of an antiseptic and 40-65 weight parts of a solvent. The invention also provides a preparation method and a use of the sodium azulene sulfonate gel. The sodium azulene sulfonate gel has the advantages of good appearance, good coating performances, use convenience, good biocompatibility with skin, no irritation and no pollution on clothes, and has strong skin adhesion, good permeability and a high concentration on local skin.
US8802717 Methods of treating arthritic conditions using (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline 1,3-dione Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (−) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4.
CN101838277A Cefotetan disodium hydrate and preparation method and application thereof The invention relates to a cefotetan disodium hydrate and a preparation method and application thereof. The cefotetan disodium hydrate has high storage stability, and is applicable to the preparation of medicines for treating or preventing diseases of the human being or animals caused by gram-positive or gram-negative sensitive bacteria, such as respiratory system diseases, hepatobiliary system diseases, five-sense organ diseases, urinary tract infection, celiac infection, pelvic infection, ichorrhemia, skin tissue infection, bone and joint infections, cephalomeningitis and endocarditis.
US20070269847 Methods, pharmaceutical formulations and kits for identification of subjects at risk for cancer Subjects at risk for developing cancer may be identified by obtaining samples of diagnostic cells from the subjects and determining a measure of cytotoxicity of the cells, the measure of cytotoxicity correlating negatively with the risk of developing cancer. The development of cancer may be prevented in subjects determined to be at risk for developing cancer by administering priming and activating agents to the subject, by increasing the expression of A1 adenosine receptors in cells of the subject, and increasing the affinity of cells of the subject for A1 adenosine receptor ligands. The preventative and diagnostic methods of the present invention may be carried out with kits and pharmaceutical liposomal formulations.
CN1850085A Medicinal composition soft capsule and its preparing method The present invention relates to amedicine composition soft capsule using famciclovir as active component and its preparation method. Said soft capsule is made up by using famciclovir, diluent, cosolvent, solubilizer, suspension adjuvant and surfactant through a certain preparation process.
US20080318989 Pyrimidine Kinase Inhibitors The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I) wherein ring A, X, Y, Z, R1, R2, R3, R4, m and n are as defined herein.
US20130052257 Antimicrobial hydrogel wound dressing The antimicrobial hydrogel wound dressing is a swellable polymer gel made from about 7-9% (wt/vol) polyvinyl alcohol (PVA), preferably 8.9%, about 0.1% (wt/vol) polyvinyl pyrrolidone (PVP), and about 1-2% (wt/vol) agar, preferably 1%, the balance (about 90%) being distilled water, the foregoing contents being crosslinked by gamma radiation at a dose of about 30 kGy. Prior to crosslinking by gamma radiation, an effective amount of a pair of antibiotics is added to the gel at room temperature. The antibiotics include about 10,000 IU of polymyxin B sulfate, and about 5 mg neomycin per gram of gel. The polymyxin provides effective protection against various forms of gram negative microorganisms, and the neomycin is a broad spectrum antibiotic that provides protection against various forms of gram positive microorganisms. The hydrogel has sufficient mechanical strength for use as a wound dressing, and is capable of absorbing water up to 900% of its volume.
US7964641 administering lipid glycerides for treating neurodegenerative disease such as multiple sclerosis; increasing transforming growth factors and tumor necrosis factors A method is provided for treating a patient in need of therapy for a neurodegenerative disease comprising administering to that patient a therapeutically effective dose of a lipid glyceride comprising a glycerol moiety and a fatty acid moiety, the fatty acid moiety being selected from the group consisting of γ-linolenic acid, dihomo-γ-linolenic acid and arachidonic acid characterized in that the selected fatty acid moiety is attached to the glycerol moiety at its sn-2 position. Preferably the method is that wherein the lipid is administered for a duration and at a dose sufficient to maintain or elevate TGF-β1 levels in the patient to therapeutic levels.
US20090239818 Effective treatment of ovarian cancer using triciribine and related compounds The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat ovarian cancer by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug. The invention further encompasses a number of miRNAs, which are altered in human ovarian cancer, with the most significantly deregulated miRNAs being miR-214, -199a*, -200a, -100, -12Sb, and let-7 cluster. Further, the invention illustrates that frequent deregulation of miR-214, -199a*, -200a and -100 in ovarian cancers and their alterations are associated with high grade and late stage tumor. Significantly, miR-214 induces cell survival and cisplatin resistance through targeting 3′UTR of the PTEN, which leads to down regulation of PTEN protein and activation of Akt pathway. Inhibition of Akt using Akt inhibitor, API-2/triciribine, or introduction of PTEN cDNA lacking 3′UTR largely abrogates miR-214 induced cell survival. These findings indicate that deregulation of miRNAs is a recurrent event in human ovarian cancer and that miR-214 induces cell survival and cisplatin resistance primarily through targeting the PTEN/Akt pathway.
US7030245 A chemical intermediate, toluene-4-sulfonic acid 7,8-dihydro-6H-5-oxa-1-aza-phenanthren-6-ylmethyl ester for preparing antidepressant, 6-[4-(5-fluoro-1H-indol-3-yl)-3,6-dihydro-2H-pyridin-1-ylmethyl]-7,8-dihydro-6H-5-oxa-1aza-phenanthrene; treating psychological disorders Compounds of the formula useful for the treatment of such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addition, sexual dysfunction (including premature ejaculation), and related illnesses.
CN101412696A 4,5-diaryl pyrazole-3-amido derivative, and preparation and use thereof The invention provides 4, 5-diarylpyrazole-3-amino derivatives. A series of the 4, 5-diarylpyrazole-3-amino derivatives are synthesized by using a natural product CA-4 as a lead compound, and using 3-aminopyrazole ring to substitute an ethylene jointed chain in a CA-4 structure as a conformation restrictive group. Pharmacological activity screening experiments show that the compounds have better antitumor activity and have better in vitro proliferation inhibiting function on various tumour cell strains, and the derivatives and the physiologically acceptable salt thereof can be applied to the preparation of antitumor drugs. The derivatives have the advantages of reasonable design, simple preparation, and practicability. The general formula of the derivative is the above one.
US20060211636 Macrolide Antibiotics The present invention relates to 11,12 γ lactone ketolides of formula (I) wherein R, R1, R2, R3 are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
EP1913937A1 Guaifenesin sustained release formulation and tablets The invention relates to a modified release pharmaceutical product having two portions, wherein a first portion comprises a first quantity of guaifenesin and a first pharmaceutical additive in an immediate release formulation, wherein the first quantity of guaifenesin becomes fully bioavailable in the subject's stomach, and a second portion comprises a second quantity of guaifenesin and a second pharmaceutical additive in a sustained release formulation, wherein the ratio of said first quantity to said second quantity provides a Cmax in a human subject equivalent to the Cmax obtained when the first of three doses of a standard immediate release formulation having one third of a total amount of guaifenesin in the modified release product is dosed every four hours over a 12 hour period, wherein said product also provides therapeutically effective bioavailability for at least twelve hours after a single dose in a human subject according to serum analysis, and wherein the total amount of guaifenesin in the modified release product is from 600 mg to 1200 mg.
CN101156916A A medicine for treating hyperpyrexia disease of pig The invention provides a medicine which can be used to effectively treat swine high fever. The drug efficacy components are produced with the raw materials in the following parts by weight: gypsum is 100 to 200 parts, scutellaria is 80 to 150 parts, dried rehmannia root is 80 to 150 parts, moutan bark is 80 to 150 parts, atractylodes rhizome is 80 to 150 parts, phellodendron bark is 80 to 150 parts, cape jasmine is 80 to 150 parts, and rhubarb is 80 to 150 parts. Together with pharmaceutically acceptable carrier, the medicine can be produced into various dosage forms, such as powder, mixture, tablets, capsules as well as granules, etc. The medicine is suitable for symptoms of damp heat accumulation, high fever, spirit depression, inappetence, cough and dyspnea, disturbance in respiration, even pneumonia, and constipation which are caused by gradual intrusion of toxic heat into nutrient and blood, and induced weak fetus, even dead fetus and mummy fetus, etc. when the toxic heat attacks pregnant pigs. The medicine has good curative effect for weanling pigs, fattening pigs and brood sows, with up to 85 percent total effectiveness rate.
US20100029597 Reca inhibitors with antibiotic activity, compositions and methods of use The present invention is directed to the use of RecA inhibitors as antibiotic agents, and provides RecA inhibitors useful in treating infections. Also provided are various compositions and methods associated with RecA inhibition.
CN1714788A Tinidazole powder injection and its preparing method The present invention discloses a kind of tinidazole powder for injection and its preparation process. It contains tinidazole in effective treating dosage, and is prepared through mixing tinidazole with beta-cyclodextrin or its derivative as the including material, adding certain amount of injection water, grinding or ultrasonic treatment to prepare clathrate aque, adding mannitol, lactose or other excipient, filtering, sterilizing, and freeze drying or spray drying. The tinidazole powder for injection has high water dissolubility, stable quality and long preservation life.
CN103690966A Self-help-feeding drug carrier for chickens and preparation method thereof The invention relates to a self-help-feeding drug carrier for chickens and a preparation method thereof. The drug carrier is composed of the following components in percentage by mass: 10-30% of pear, 12-25% of corn flour, 0.4-8% of carrageenin, 5-15% of bean pulp powder, 4-8% of honey, 0.2-0.5% of table salt, 0.1-2% of vitamin complex, 0.1-2% of composite mineral, 0.02-0.05% of potassium sorbate and 37-68% of water. The product is suitable for directly feeding, and is used for preventing and treating common clinical diseases of chickens to achieve the dual effects of preventing and treating diseases and strengthening the constitution; and the drug carrier has the advantages of favorable palatability and the like, can implement self-help feeding, is convenient to use, and solves the problems of labor and time consuming, animal stress reaction, pains and the like caused by oral administration or injection administration. Besides, the product has the advantages of simple production technique, wide raw material sources and low production cost, and is suitable for large-scale production.
CN103463011A Application of fluevirosines A in preparation of medicine inhibiting liver fibroblast proliferation The invention discloses the application of fluevirosines A in preparation of the medicine inhibiting liver fibroblast proliferation. The pharmacological test shows that the fluevirosines A can inhibit generation and development of liver fibrosis obviously and can be used for preparing the medicine for preventing liver fibrosis and preventing and curing liver cirrhosis. The fluevirosines A belongs to a brand new matrix type, has the advantages of being high in inhibitory activity to liver fibroblast proliferation and prominent in substantive features, and makes remarkable progress in prevention of liver fibroblast proliferation.
CN102973581A Use of madecassoside of centella asiatica in preparing medicaments for treating liver fibrosis The present invention relates to the use of centella asiatica, and in particular relates to the use of monomer madecassoside of the centella asiatica in preparing medicaments for treating liver fibrosis. The present invention also provides madecassoside injection for the treatment of liver fibrosis and preparation method thereof. The present invention effectively broadens choices of liver fibrosis and cirrhosis patients, and compared with existing medicaments for treating liver fibrosis, the products of the present invention has the advantages of good efficacy, and little adverse side effect.
CN101199530A Itraconazole nanometer suspensions lyophilized compound and preparing , using method thereof The invention discloses a freeze-drying combination of itraconazole nanosuspension for injection and preparation and using methods of the nanosuspension. The invention selects serum albumin of the human as main adjunct; itraconazole nano-sized granulation can be successfully realized by adopting the drying technology and freeze drying technology in combined liquid of high pressure homogenization nanometer emulsification technology; and the invention can be filtered to sterilize and can be stored in the form of freeze-dried powder. The itraconazole nanosuspension is prepared in acceptable waterborne diluent in pharmacy, and then the average particle size of the itraconazole nanosuspension is less than 0.3 microns after reconstruction, so the itraconazole nanosuspension can be made into nanosuspension for intravenous injection. The nanosuspension is composed of the following components : the ratio between the itraconazole and albumin is 1 : 200 to 10 : 1; and the nanosuspension also comprises surfactant, stent agent, osmo-regulator and other injection additives, etc. The nanosuspension has the advantages of drug loading, safety, low toxicity, high stability and good warming promotion without hemolysis or stimulation on vein vascular. And the preparation method is simple and easy, and thus the product forming can be realized easily.
CN101214378A Yam polysaccharide complex immunity globulin anti-infectious preparations and preparation thereof The invention discloses a Chinese yam polysaccharide composite immunoglkobulin anti-infective preparation and a preparation method thereof, and relates to the field of food and food manufacturing. The components and the weight portions of the components are as below: Chinese yam polysaccharide 0.01 to 100.0, immunoglkobulin 1.00 to 100.0. The Chinese yam polysaccharide is extracted from Chinese yam, and the immunoglkobulin is yolk immunoglkobulin prepared by purification from the yolk of poultry eggs. 0.5 percent to 10.0 percent of the preparation is directly added into foods or drinks, to benefit spleen qi and improve the human immunity. The Chinese yam polysaccharide composite immunoglkobulin anti-infective preparation fully embodies the combination of the TCM theory and the current immunololgy, and is a brand-new and high-efficiency condensed food of effectively exciting and regulating the organism immune functions.
CN101353339B Synthesis of quercetin platinum The invention relates to quercetin which has multiple aspects of biological activities, and has effects of phlegm elimination, asthma relief and antiatheroscloresis, etc., and has activities of fighting against the hyperplasia of various tumor cells; platinum complexes have obvious anticancer effect and the combination use of the quercetin and the cisplatin results in synergistic effects. In the invention, the quercetin reacts with a platinum compound under a certain condition for obtaining a quercetin platinum complex by being subjected to reversion, distill, chromatography and separation. The results from the MIT method experiment show that the quercetin platinum significantly inhibits the cell proliferation of tumors such as hepatoma HepG2, cervical carcinoma Hela and laryngocarcinoma Hep2, etc.
US20110045102 Cancer chemotherapy compositions comprising PI3K pathway modulators and triptolide The present invention provides compositions and methods for inhibiting growth of and/or killing cancer cells. The compositions include: an inhibitor of the PI3K signal transduction pathway, and additional agents, such as Triptolide.
CN103054844A Application of GW3965 in preparation of drugs treating or preventing hepatitis C The invention discloses application of GW3965 (3-[3-[[[2-chloro-3-(trifluoromethyl)phenyl]methyl](2, 2)-biphenylethyl)amino]propoxy)phenylacetate hydrochloride) in preparation of drugs treating or preventing hepatitis C virus. A drug without any toxic concentration is chosen for an antiviral experiment, the influence of GW3965 on virus gene duplication is detected, and results show that the small molecule compound has significant antiviral activity and is dose dependent. Then, the GW3965 is employed to treat the hepatitis C pseudovirus system of different gene subtypes, and results show that the compound inhibits the virus entrance link at the early stage of a virus lifecycle. The anti-virus capability of drug combination of GW3965 and other anti-HCV drugs is detected, and results show that the compound has the potential of drug combination with other drugs. GW3965 can inhibit 1a, 1b, and 2a genotype virus entrance, and has broad-spectrum antiviral activity and a novel target, while there is no anti-hepatitis C virus drug with entrance as the target clinically. And drug combination can achieve a good effect.
CN101027058A Cancer combination therapy comprising AZD2171 and imatinib The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionizing radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumor or a leukaemia, which comprises the administration of AZD2171 in combination with imatinib; to a pharmaceutical composition comprising AZD2171 and imatinib; to a combination product comprising AZD2171 and imatinib for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and imatinib; to the use of AZD2171 and imatinib in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionizing radiation.
CN101190944A Human cytokine and use thereof The invention discloses a new secretive cytokine NS128 of human beings, which relates to a coding amino acid sequence of the cytokine or the polynucleotide of the cytokine fragment, containing a genetic engineering carrier and a host cell of the polynucleotide. The invention also relates to a production method of the amino acid sequence of the cytokine or the polypeptide of the cytokine fragment and the production method of the polypeptide as well as a small interference RNA, which suppresses the expression of the cytokine. The invention also relates to a salt which contains the polynucleotide or the salt of acceptable drugs, or a medical composition of the polypeptide or the salt of acceptable drugs. The invention further relates to applications of the polynucleotide of the cytokine, the polypeptide or the small interference RNA in preparation of prevention and/or treatment medicines for tumor, infection, hematopoietic disorder and autoimmune disease, etc., in particular having clinical implications for tumor, inflammation and nervous system disease and so on related to MAPK signal pathway. The invention also relates to a method of in vitro testing whether the expression of the polynucleotide or the polypeptide changes. The invention also relates to a monoclonal or polyclonal antibody which is specifically bound with the polypeptide or an active fragment of the polypeptide.
US20120225873 Compounds for alzheimer's disease The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH, -L-C(═O)NH2, -L-C(═O)NH(C1-3 alkyl), -L-C(═O)N(C1-3 alkyl)2, -L-S(═O)2(C1-3alkyl), -L-S(═O)2NH2, -L-S(═O)2N(C1-3 alkyl)2, -L-S(═O)2NH(C1-3 alkyl), -L-C(═O)NHOH, -L-C(═O)CH2NH2, -L-C(═O)CH2OH, -L-C(═O)CH2SH, -L-C(═O)NHCN, -L-NHC(═O)ORo, -L-C(═O)NHRo, -L-NH(C═O)NHRo, -L-C(═O)N(Ro)2, -L-NH(C═O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
CN102199148A Benzsulfamide derivatives and medicinal composition thereof The invention relates to benzsulfamide derivatives and a medicinal composition thereof. The benzsulfamide derivatives are shown as a formula (I), wherein R1, R2, R3 and D are defined as the description. In addition, the benzsulfamide derivatives can serve as cell cycle inhibitors, so the benzsulfamide derivatives and the medicinal composition thereof can serve as cell cycleanti-cancer medicines. The benzsulfamide derivatives can particularly serve as anti-cancer medicines for treating solid tumors.
CN103214444A Flavone sulphonamide derivative with anti-cancer activity as well as preparation method and application thereof The invention discloses a flavone sulphonamide derivative with anti-cancer activity as well as a preparation method and an application thereof. The derivative is a compound with a structural formula shown as a general formula I or pharmaceutically acceptable sodium salt, potassium salt, sulphate, hydrochloride, a halogen compound or an ester compound of the compound shown in the general formula I; the derivative is simple and practicable in preparation method and low in cost; and the derivative disclosed by the invention has good anti-tumour activity, obvious inhibition effect to a HepG2 human liver cancer cell strain and good practical value and application prospect in the filed of preparation of anti-tumour drugs.
CN103550185A Neomycin sulfate effervescent tablet for veterinary use as well as preparation method thereof The invention discloses a neomycin sulfate effervescent tablet which consists of the following components: neomycin sulfate as a medicinal component, tartaric acid and sodium hydrogen carbonate as effervescing agents, PVP (Polyvinyl Pyrrolidone) k30 and soluble starch as adhesives, talcum powder as a lubricant, auxiliary US powder as a filling agent, and low-substituted hydroxypropyl cellulose as a disintegrating agent. The neomycin sulfate effervescent tablet disclosed by the invention has the beneficial effect that a local medicine delivery path of intrauterine delivery is adopted, so that the neomycin sulfate effervescent tablet has a great targeting effect. Due to the characteristic that the effervescent tablet encountered with water generate bubbles, the medicine is uniformly delivered to endometrium comprising endometrium wrinkles, so that the medicine distribution area is expanded, and the medicine can be in full contact with inflammations in the endometrium to exert a treatment effect to a greater extent. Tests verify that the treatment effect of the neomycin sulfate effervescent tablet disclosed by the invention is superior to that of a conventional neomycin sulfate tablet. The preparation method of the neomycin sulfate effervescent tablet disclosed by the invention is good in repeatability, and in the production process, no sticking and cracking are generated, so that the effervescent tablet prepared is smooth in surface, high in hardness and great in effervescent amount, and can meet the clinical demands of veterinarians.
EP2035092A2 Use of kw-3902 for achieving diuresis in patients with congestive heart failure and acute fluid overload Methods of treating patients with acute fluid overload comprising administering diuretic therapy and an amount of KW-3902, a pharmaceutically acceptable salt, ester, amide, metabolite, or prodrug thereof, effective to accelerate removal of excess fluid from the patient in comparison to diuretic therapy alone. Methods of improving the treatment time to achieve adequate diuresis in an individual experiencing acute fluid overload comprising administering to said individual a diuretic and a therapeutically effective amount of KW-3902 or a pharmaceutically acceptable salt, ester, amide, metabolite, or prodrug thereof.
EP1469743A4 Stable hygroscopic compositions and methods for stabilizing hygroscopic ingredients The present invention provides methods and compositions for providing controlled protection for hygroscopic ingredients that will be exposed to moist or humid environments for significant periods of time by encapsulating the hygroscopic ingredients with a controlled-protection lipid coating. The methods and compositions are particularly useful for stabilizing a hygroscopic bioactive substance, such as choline or lysine hydrochloride, in an animal feed composition and also providing adequate rumen protection in ruminant feeds.
US20080261999 Azabicycloalkane Derivatives Useful as Nicotinic Acetylcholine Receptor Agonists Compounds of the formula I or a pharmaceutically acceptable salt thereof: processes for their preparation, pharmaceutical compositions which contain them and their uses in therapy.
US7432256 Substitued imidazo [1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, —O(CH2)mO(CH2)mOH or —C≡C—R′; R2 is hydrogen or methyl; R3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, —(CH2)n-cycloalkyl, —(CR′R″)m—CH3, phenyl that is unsubstituted or substituted by halogen, pyridinyl or thienyl each of which is unsubstituted or substituted by lower alkyl, —(CH2)n—NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR′R″)mOH, or lower alkynyl-phenyl wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy; R′ is hydrogen or lower alkyl; R″ is hydrogen, hydroxy or lower alkyl; n is 0, 1 or 2; m is 1, 2 or 3; and o is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites. Thus, the invention also relates to methods of enhancing cognition and treating cognitive disorders like Alzheimer's disease.
US20090149440 1-(6-Amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-isopropylaminoazetidin-1-yl)-8-methyl-4-oxo-1,4-dihydroquinolin-3-carboxylic acid; antibacterial agent; low toxicity, improved bioavailability, and low binding rate to serum proteins The present invention provides an agent which exhibits excellent antibacterial activity, low toxicity, improved bioavailability, and low binding rate to serum proteins. The present invention is directed to a pyridonecarboxylic acid derivative represented by formula (1): or a salt thereof, wherein R1 represents a methyl group, a fluorine atom, or a chlorine atom; R2 represents a hydrogen atom or a lower alkyl group; R3 represents an isopropyl group or a tert-butyl group; R4 represents a methyl group or a halogen atom; and R5 represents a fluorine atom or a chlorine atom. The present invention is also directed to an antibacterial agent and a medicament containing the derivative or the salt thereof as an active ingredient.
WO2012041227A1 Tetracyclic heterocycle compounds for treating hepatitis c viral infection Tetracyclic heterocycle compounds of formula (I) and pharmaceutically acceptable salts thereof are provided, wherein A, A', G, R1, R15, U, V, V', W, W, X, X', Y and Y' are as defined in the invention. The pharmaceutical compositions comprising these compounds and the use of the compounds for treating hepatitis C virus (HCV) infection are also provided.
US20080274995 Suppression of Nuclear Factor-KappaB Dependent Processes Using Oligonucleotides Antisense oligonucleotides which hybridize with nuclear factor-κB (NF-κB) mRNA and methods of using these oligonucleotides.
US8263567 A lipophilic anthracycline with a pharmaceutically acceptable carrier for topical administration to a body surface and which has a higher lipophilicity than doxorubicin; valrubicin applied to mucous membranes; psoriasis; side effect reduction; not doxorubicin, daunorubicin, epirubicin or idarubicin The present invention relates to pharmaceutical formulations comprising an anthracycline and the uses thereof for treatment of clinical conditions of body surfaces such as skin and mucosal membranes, wherein abnormal cell differentiation and/or hyperproliferation is a primary factor of the pathogenesis. In particular the invention relates to treatment of psoriasis, and preferably to treatment of psoriasis with valrubicin topically applied.
CN102049016A Externally applied medicine for treating rheumatoid arthritis The invention relates to a formula of an externally applied medicine for treating rheumatoid arthritis, which belongs to the field of sanitation and daily chemicals. The externally applied medicine is characterized by being prepared from divaricate saposhnikovia root, tree peony bark, ephedra herb, frankincense and the like, and the formula comprises 30-50g of the tree peony bark, 15-45g of the ephedra herb, 50-70g of the frankincense, 300-600ml of white spirit, 20g of ginger and 4-7g of red jujube. The externally applied medicine is not only sanitary, but also practical, thus the formula of the externally applied medicine is more ideal for treating and controlling the rheumatoid arthritis.
CN102764237A Oral enteric-coated pellet medicinal preparation The invention discloses an oral enteric-coated pellet medicinal preparation. The preparation comprises a plurality of enteric-coated pellet units; each enteric-coated pellet unit comprises a compound serving as an active ingredient; the compounds are at least one of omeprazole, omeprazole salt, (-)- omeprazole enantiomer and (-)- omeprazole enantiomer salt; the enteric-coated pellet medicinal preparation consists of pill cores comprising the active ingredients and adhesives, isolation layers comprising isolation components and enteric-coated layers; the pill cores are separated from the enteric-coated layers by the isolation layers of enteric-coated pellets; according to the adhesives in the pill cores and/ or the isolation components in the isolation layers, polyvinyl alcohol/ polyethylene glycol (in a ratio of 3:1) graft copolymer is used; the enteric-coated pellets and other excipients are mixed and pressed into tablets, or the enteric-coated pellets are filled into capsules. The oral enteric-coated pellet medicinal preparation has the advantages that the problem that the omeprazole is easy to degrade or transform in an acidic or neutral medium is solved; and the polyvinyl alcohol/ polyethylene glycol (in a ratio of 3:1) graft copolymer has positive influence on the stability of the preparation.
US20080219968 Son of sevenless homolog 1 (SOS1) suppressive agent for prevention and treatment of cell proliferative disorders Inhibitors of human Sos1, including antisense oligonucleotides, methods, and compositions specific for human Sos1, are provided. Methods of using the compositions for modulating Sos1 expression and for regulating cell growth, particularly tumor cell growth, are also provided.
US20080103134 Use of selected CGRP-antagonists in combination with other antimigraine drugs for the treatment of migraine The present invention relates to a process for the treatment or prevention of indications which are selected from among the group comprising headaches, migraine and cluster headaches, this process comprising the joint administration of a therapeutically effective amount of a selected CGRP antagonist (A), a physiologically acceptable salt thereof or a hydrate of the salt and a therapeutically effective amount of a second or third active anti-migraine medicament (B), particularly sumatriptan, zolmitriptan or dihydroergotamine or a physiologically acceptable salt thereof, and to the corresponding pharmaceutical compositions and the preparation thereof.
US6849655 Aqueous liquid formulations An aqueous liquid formulation which comprises a compound of formula I: wherein Y is a hydroxy group, a carboxyl group, an acyloxy group or an alkoxycarbonyl group; R is a lower alkyl group or a lower alkyl group with one or more halogen atoms; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate of them as an active ingredient, together with one or more substances selected from the group consisting of boric acid, borax, phosphate salts and carbonate salts.
EP2289892A1 Maleimide derivatives, pharmaceutical compositions amd methods for treatment of cancer The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention.
CN101530520A Deflocculat suppository powder The invention discloses a deflocculat suppository powder, which is prepared by mixing water decoction solution with 5-40g of omphalia powder and 25-35g of sodium bicarbonate solution, wherein the water decoction solution is prepared by mixing and decocting 5-30g of rhizoma alismatis, 6-35g of hemlock parsley, 10-30g of safflower, 10-30g of processed radix aconiti lateralis and 15-35g of salvia miltiorrhiza. The deflocculat suppository powder can fully dissolve 1.2cc of coagulated blood clots of human body within 32h, the time is 176h less than the time for which Buchang Naoxintong can fully dissolve 1.2cc of coagulated blood clots of human body, and the speed for dissolving the coagulated blood clots is greatly increased. And in the application to the clinical treatment of eyeball and cardiovascular and cerebrovascular diseases of human body, the deflocculat suppository powder does not generate any bad reaction and has high safety. Simultaneously, the deflocculat suppository powder can also be used for dissolving the coagulated blood clots of animal body and fully dissolve 1.2cc of edible boiling pig blood clots for average 152h, which is 56h less than the time needed by Buchang Naoxintong to fully dissolve 1.2cc of coagulated blood clots of human body.
US20120183502 Combination therapy for lysosomal storage diseases This invention provides various combinations of enzyme replacement therapy, gene therapy, and small molecule therapy for the treatment of lysosomal storage diseases.
US20130018012 Lipid composition for improving brain function The invention pertains to the use of a lipid fraction for the support of brain function. The lipid fraction comprises the medium-chain fatty acids at least 4 g hexanoic acid and/or at least 5 g octanoic acid, at least 1 g eicosapentaenoic acid, and in addition more than 0.4 g α-linolenic acid per 100 g fatty acids of the lipid fraction.
WO2014157966A1 Pharmaceutical composition for preventing or treating ovary granulosa cell tumors containing glycogen synthase kinase-3 beta inhibitor as active ingredient, and functional health food composition The present invention relates to a pharmaceutical composition for preventing or treating ovary granulosa cell tumors containing, as an active ingredient, one selected from the group consisting of a compound represented by chemical formula 1, a pharmaceutically acceptable salt of the compound represented by chemical formula 1, a compound represented by chemical formula 2, and a pharmaceutically acceptable salt of the compound represented by chemical formula 2, or a functional health food composition. The composition according to the present invention inhibits glycogen synthase kinase-3 beta (GSK3beta) and thus has an effect of inhibiting a phosphorylation of serine, which is the 33rd amino acid of the forkhead box L2 (FOXL2) protein, by containing, as an active ingredient, one selected from the group consisting of the compound represented by chemical formula 1, the pharmaceutically acceptable salt of the compound represented by chemical formula 1, the compound represented by chemical formula 2, and the pharmaceutically acceptable salt of the compound represented by chemical formula 2, so that the composition can be useful as a composition for preventing or treating ovary granulosa cell tumors. Further, the composition according to the present invention is expected to be also useful as a functional health food composition.
WO2008075796A1 Agent for promoting recovery from blood cell depletion Disclosed are a means and a method useful for the promotion of the recovery from blood cell depletion. Specifically disclosed are: (a) R-spondin 2 or 3 protein; (b) a nucleic acid encoding R-spondin 2 or 3 protein; (c) an expression vector carrying a nucleic acid encoding R-spondin 2 or 3 protein; and (d) an agent for promoting the recovery from blood cell depletion, which comprises at least one cell transformed with a nucleic acid encoding R-spondin 2 or 3 protein or an expression vector carrying the nucleic acid.
CN101543509A Ophthalmic gel containing chondroitin sulfate and method for preparing same The invention relates to an ophthalmic gel containing chondroitin sulfate and a method for preparing the same. The ophthalmic gel comprises chondroitin sulfate and taurine in effective dose and an aqueous gel substrate in proper amount. Compared with eyedrop, the ophthalmic gel has the advantages of good biocompatibility, small stimulation, simple preparation process and the like.
WO2009132202A3 Macrocyclic compounds and their use as kinase inhibitors The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
CN1559435A Oral liqid-supplement salt effervesce tablets, and prepn. method therefor An orally-applied ffervescent tablet for supplementing salt to human body is prepared from sodium chloride, sodium citrate, potassium chloride, anhydrous glucose, dicarbonate, and pregelatinized starch through baking pregelatinized starch anddicarbonate, sieving others, proportional mixing, andtabletting.
WO2010117756A3 Substituted benzimidazole pharmaceutical formulations Stable pharmaceutical compositions of dexlansoprazole with pharmaceutical excipients, processes for preparing the stable compositions, packaging and their use in treatment of erosive esophagitis and heartburn associated with non-erosive gastroesophageal reflux disease.
US20120108563 Methods Of Treating Liposarcoma Provided herein are methods of treating liposarcoma in a subject, the method comprising administering to the subject a therapeutically effective amount of an Hsp90 inhibitor.
WO2011150098A1 Compositions and methods for reduction of mercury toxicity Provided are compositions containing melatonin and zinc. Additionally provided are dosage forms containing the compositions, and methods of making the compositions and dosage forms. Methods of removing mercury from the body of subject are provided, as are methods of treating and/or preventing certain conditions associated with mercury toxicity.
US20110142930 Pharmaceutical Compositions of Atorvastatin A dry-granulated pharmaceutical composition comprising atorvastatin or a pharmaceutically acceptable salt thereof, as well as a dry-granulated pharmaceutical composition comprising atorvastatin or a pharmaceutically acceptable salt thereof in combination with at least one other active drug, methods for preparing said compositions, kits for containing such compositions, and a method of treating hypercholesterolemia and/or hyperlipidemia, osteoporosis, benign prostatic hyperplasia (BPH), and Alzheimer's disease using a therapeutically effective amount of the pharmaceutical composition.
WO2008151412A1 Synergistic inhibition of h1n1 and h3n2 influenza viruses by aurintricarboxylic acid with amantadine Treatment of influenza virus infections by administering to an individual, for example, an effective amount of aurintricarboxylic acid (ATA) is herein described. In some embodiments, ATA is co-administered with amantadine, the combination having synergistic effects.
WO2009110519A1 Novel 1-aminocarbonylpiperidine derivative Disclosed is a novel compound useful as an antiallergic agent, namely a novel 1-aminocarbonylpiperidine derivative represented by formula (I) or a physiologically acceptable salt thereof. (In the formula, ring A represents an azetidin-1-yl group, a pyrrolidin-1-yl group, a piperidino group, a piperazin-1-yl group, a morpholino group or the like; R1 represents an optionally substituted phenyl group, an optionally substituted C3-8 cycloalkyl group or the like; R2 represents an optionally substituted phenyl group or the like; R3 and R4 may be the same or different and each represents a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group or the like; and m represents 1, 2 or 3.)
US20080171738 Administering a methylol-transferring antiproliferative agent taurolidine, taurultam or a mixture in dosing cycles of an administration phase of daily dose for 1-8days followed by a non-adminstration (rest) phase of 1-14 days; infusion; before or after suregical removal; antitumor, -carcinogenic agents A method of treating a patient with breast cancer includes administering to the patient a breast cancer cell proliferation-inhibiting amount of a methylol-containing compound such as taurolidine, taurultam or a mixture thereof.
US20110118312 Benzylpiperizine compound Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.)
CN103191360A Hippocampal hedgehog pill The invention discloses a hippocampal hedgehog pill, comprising 1 hippocampi, 60g of placenta hominis, 30g of concha mauritiae, 30g of oyster, 60g of concha haliotidis, 30g of actinolite, 60g of keel, 60g of rhizoma curculiginis, 60g of folium mori, 30g of common cnidium fruit, 30g of hedgehog hide, 60g of morinda officinalis, 15g of fructus amomi, 15g of fructus alpiniae oxyphyllae, 60g of semen cuscutae, 60g of sea cucumber, 30g of donkey-hide gelatin, 30g of deer-horn glue, 60g of longspur epimedium, 30g of tag, 30g of white atractylodes rhizome, 30g of jilin ginseng, and 90g of cherokee rose fruit. The medicines are grinded into fine powder; 300g of Chinese yam is pasted into pills; a 10g of pill is taken in the morning and evening in everyday, and eaten by plain boiled water; sexual intercourse is prohibited; in addition, 20g of gallnut is utilized to decoct for half an hour by a slow fire; proper warm boiled water is added; the penis glans is fumigated for a few minutes when being hot; the glans penis is soaked in the medicine liquor for 5-10 minutes when the water temperature is about 40 DEG C, and the process is repeated for a plurality of times in the morning and evening; 15-20 days are taken as a treatment course; and the hippocampal hedgehog pill is taken for 2-3 treatment courses in general, and mainly used for treating premature ejaculation.
US20120121720 Modulation of Beta 2 Adrenergic Receptors by Inhibitors of EGLN3 or pVHL This present invention relates to methods, compositions, and kits useful for treating a patient having or at risk for developing a disorder associated with decreased expression of β2 adrenergic receptors or need for increased 132 adrenergic receptor activity.
EP1280555B1 Pharmaceutical composition comprising furosemide and conivaptan for the treatment of congestive heart failure Combinations of diuretics and vasopressin antagonists are useful to slow and reverse the symptoms and process of congestive heart failure, to increase the excretion of water in the urine, and to decrease the excretion of sodium and potassium ions in urine. Preferred vasopressin antagonists have the formula (I) wherein R and R5 are hydrogen or lower alkyl; R?1, R2, and R3¿ are hydrogen, halo, alkyl, alkoxy, and amino; and R4 is hydrogen or phenyl, and a pharmaceutically acceptable salt thereof.
US7855199 antitumor agents such as 2-(2-difluoromethyl-4-methoxybenzimidazol-1 -yl)-4-(cis-2,6-dimethylmorpholino)-6-morpholinopyrimidine, used for inhibiting the growth of a human colon cancer cell, a human lung cancer cell, a human breast cancer cell or a human prostate cancer cell Heterocyclic compounds represented by the formula I and anti-malignant-tumor agents containing the heterocyclic compounds as effective components: wherein X represents nitrogen atom or CH; Y represents C1-C6 alkyl; R1 represents morpholino (which may be substituted with one to four C1-C6 alkyl); and R2 and R3 each represent hydrogen atom or C1-C6 alkyl.
CN103169704A Compound slow-release capsule preparation of nicotinic acid and simvastatin as well as preparation method of preparation The invention provides a capsule containing a nicotinic acid slow-release tablet and a simvastatin mixture. The compound slow-release capsule preparation includes the nicotinic acid slow-release tablet and the simvastatin mixture, wherein the content of the nicotinic acid is 50%-80%. The simvastatin mixture includes the simvastatin and other medical auxiliary materials, wherein the content of the simvastatin is 20%-80%. The invention provides the preparation method of the compound slow-release capsule preparation of nicotinic acid and simvastatin. The preparation method comprises the following steps of: preparing the simvastatin and the medical auxiliary materials into a simvastatin mixture; preparing the nicotinic acid and the medical auxiliary materials into a slow-release tablet; filling the simvastatin mixture to the capsule by using a capsule filling machine; filling the nicotinic acid slow-release tablet to the capsule to obtain the nicotinic acid-simvastatin slow release capsule. The compound slow-release capsule preparation disclosed by the invention is good in stability, controllable in quality, simple in preparation method, suitable for industrial production and large in application value.
US8106068 Compositions and methods for modulating c-kit and PDGFR receptors The invention provides compounds of Formula (2), and pharmaceutical compositions thereof, wherein R1, R2, R3, R4 and L are as described herein; as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFRα, PDGFRβ, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.
CN103203020A Application of statin medicines in preparing medicines used for treating chronic subdural hematoma The invention discloses an application of statin medicines in preparing medicines used for treating chronic subdural hematoma (CSDH). The application provided by the invention has the advantages that: 1, the safety is high; the medicine does not cause severe complications; CSDH reoccurrence is prevented for a long time after applciation; and an effect is reliable; 2, medication is convenient and is easy to be accepted by patients, wherein the medicine needs to be taken only once a day, and an amount is appropriate, such that patient daily lives are not affected; 3, the medicine is economical, wherein the medicine can be orally taken at home, such that hospitalization costs, surgical treatment costs, and care worker costs before and after surgery are avoided; and 4, defects such as anesthesia risk, pain risk, surgical bleeding, brain physiological cycle disruption, brain function damage, postoperative infection and recurrence, and the like of a traditional borehole drainage operation used for treating CSDH are avoided.
WO2014009296A1 Imidazopyrazine derivatives as modulators of tnf activity A series of imidazo[1,2-α]pyrazine derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
CN103494804A Application of Neonectrolide A in preparing antibacterial drugs The invention relates to application of Neonectrolide A in preparing antibacterial drugs. The Neonectrolide A has a strong inhibition function on escherichia coli, pseudomonas fluorescens, staphylococcus aureus, proteusbacillus vulgaris and cryptococcus neoformans, can be used as a compound with an antibacterial function, and is public for the first time. The Neonectrolide A is strong in bacteriostasis activity, has the advantage of being prominent in substantiality, and meanwhile has significant progress in preventing and treating bacterial infection.
CA2842362A1 Hydrazide containing nuclear transport modulators and uses thereof The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
US7119207 NK-1 receptor antagonists, (e.g., substance P receptor antagonists) The present invention relates to certain benzoamide piperidine containing compounds and related compounds that exhibit activity as NK-1 receptor antagonists, (e.g., substance P receptor antagonists), to pharmaceutical compositions containing them, and to their use in the treatment and prevention of central nervous system disorders, inflammatory disorders, cardiovascular disorders, ophthalmic disorders, gastrointestinal disorders, disorders caused by helicobacter pylori, disorders of the immune system, urinary incontinence, pain, migraine, emesis, angiogenesis and other disorders.
US8003638 7-pyrazolylbenzazepines having affinity for D3 receptor Compounds of formula (I) or a salt thereof are disclosed: wherein R1 is pyrazolyl substituted by two or three substituents independently selected from halogen, C1-4alkyl and haloC1-4alkyl; R2 is hydrogen or methyl; and R3 is quinolinyl, oxazolyl or phenyl, each of which is optionally substituted by one or two halogen, C1-4alkyl or haloC1-4alkyl. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.
WO2008072682A1 Imidazo[1,2-b]pyridazine derivative A novel low molecular compound which has an action of inhibiting TNF-α production, exerts an excellent effect in a pathological model of inflammatory disease and/or auto-immune disease, has high safety, and can be orally administered is provided. A compound represented by the following general formula (I): [wherein R1 represents a hydrogen atom or a C1-C6 alkyl group, R2 represents a C1-C6 alkyl group which may have a substituent or the like, the ring A represents a benzene ring or the like, X represents a hydrogen atom or 1 to 3 groups, which may be the same or different, selected from the group consisting of a halogeno group, a C1-C6 alkyl group and the like, and Y represents a group represented by -N(R3a)C(R6aR7a)C(R8aR9a)N(R4aR5a) or the like, (R3a, R4a, R5a, R6a, R7a, R8a and R9a may be the same or different and represent a hydrogen atom, a C1-C6 alkyl group or the like)], a salt thereof or a solvate thereof, and a TNF-α production inhibitor comprising the compound, a salt thereof or a solvate thereof as an active ingredient.
US7456186 Diphenylimidazopyrimidines as inhibitors of β-secretase The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated β-amyloid deposits or β-amyloid levels in a patient.
US20120283295 Indazole derivatives and their use for blockading voltage dependent sodium channels The invention provides an indazole derivative of formula (1), or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1, R2, R3 and R4 are as defined herein. The indazole derivatives are capable of blockading voltage dependent sodium channels and they are useful in the treatment or prevention of normal tension glaucoma, multiple sclerosis, a motorneurone disease, stroke, spinal cord injury, Alzheimer's disease, Parkinson's disease or pain.
CN103462937A Preparation method of spansules containing large dosage of nicotinic acid The invention discloses a preparation method of spansules containing large dosage of nicotinic acid, aiming to provide a preparation method of spansules which are high in nicotinic acid content, are ideal in slow-release effect, are simple in production process, and are good in reproducibility. The preparation method of the spansules sequentially comprises the following steps of (1) pretreating original auxiliary materials; (2) mixing the original auxiliary materials and premixed powder together, placing blank pill cores into a coating granulator, adding the premixed powder into a charging hopper, additionally spraying 5% hydroxypropyl methylcellulose solution, and preparing pill cores containing nicotinic acid by a lamination method; (3) preparing a coating liquid, taking 18-20-mesh pill cores containing nicotinic acid, placing into the coating granulator, spraying the coating liquid, meanwhile spraying talcum powder on the pill cores containing nicotinic acid at the speed of 0.6g-1.4g/min, and stopping spraying the talcum powder when spraying of the coating liquid is finished, thereby obtaining the coated medicine pills; (4) mixing the coated medicine pills together after thermal treatment; and (5) filling the capsules according to the percentage content of nicotinic acid in the coated pills. The preparation method of the spansules containing large dosage of nicotinic acid belongs to the technical field of medicine preparation.
CN103221060A Tumor growth controlling method targeting galactosylceramide expression factor-1 Disclosed are an antitumor agent and a tumor growth controlling method, each has anti-angiogenic activity and/or tumor growth inhibitory activity. Specifically disclosed is an antitumor agent which contains a polypeptide that comprises at least the C region or a part thereof among the polypeptides of a galactosylceramide expression factor-1 excluding the Q region. The antitumor agent is characterized by having anti-angiogenic activity and/or tumor growth inhibitory activity.
EP2640722A1 Pyrazolopyridines and pyrazolopyridines and their use as tyk2 inhibitors The invention provides compounds of Formula (I), stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula (I) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as TYK2 Kinase inhibitors.
CN101560232A Method for preparing improved decitabine The invention discloses a method for preparing improved decitabine (formula I), comprising: using 1-alpha-chlorine-3,5-two pairs of halo-benzoyl-2-deoxidation-D-ribose (formula II) as materials, concentrating with 2-4-bi-(trimethyl silicane)-5-azacytosine (formula III) to obtain I by de-protecting group. Materials used in the invention are easy to obtain at a low price. The invention also has the advantages of convenient operation and a high reaction yield, and is suitable for industrialized production.
WO2011060065A3 Instillation of liposomal formulation of sirna and antisense oligonucleotides A pharmaceutically acceptable deliverable composition and methods for administration of macromolecules for sequence-specific gene-silencing in bladder to treat overactive bladder (OAB), interstitial cystitis/painful bladder syndrome (IC/PBS), lower urinary tract symptoms (LUTS) locally in the bladder, or other diseases or disorders of the bladder or LUTS, has been discovered, In the preferred embodiment, a liposome based delivery system is used to deliver an effective amount of antisense oligonucleotides (ODN) or siRNA that interact with or bind to messenger RNA (mRNA) coding for human nerve growth factor (NGF) to stop the synthesis of NGF.
US7147876 comprises Aloe vera, Vitamins, mineral concentrate, organic oils concentrate, Chinese herb, essential oil and spice; for medicinal/cosmetic use A medicinal or cosmetic composition comprising Aloe vera in combination with at least one vitamin, a minerals concentrate, an organic oils concentrate, at least one Chinese Herb, at least one essential oil and at least one spice. The composition may be administered orally or topically.
US20080193563 Harnessing wnt signaling to restrict hiv replication Activation of the Wnt signaling pathway potently restricts HIV replication both in peripheral blood mononuclear cells (PBMCs) and astrocytes. Inducing Wnt signaling, leading to the activation of β-catenin, for example, by the addition of lithium chloride (LiCl) inhibited the replication of a number of HIV isolates in PBMCs. Activating Wnt signaling, either with LiCl or other agents that target this pathway, is an approach to inhibit HIV replication.
US20090137549 Novel compounds useful for the treatment of degenerative & inflamatory diseases The present invention relates to compounds that are inhibitors of PDE1A, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation.
US7476740 Monoamine transporter inhibitors; used for early diagnosis and treatment of neurological and psychiatric conditions The present invention provides novel tropane compounds and methods for their use.
CN102633815A Cefoxitin esterified prodrug compound and oral preparation thereof The invention discloses a cefoxitin esterified prodrug compound and salified compound and oral preparation thereof, wherein the esterified prodrug comound shown as the following structural formula (I) contains cefoxitin serving as an active constituent. The esterified prodrug compound can exist in a manner of salt. Methyl trimethylacetate which is lipotropy perssad is introduced on the basis of cefoxitin to esterify carboxyl to obtain esterified prodrug, and bulk pharmaceutical chemicals in a modified drug form are provided. Pain of patients taking the oral preparation orally is reduced during injection, the requirement on professional institutions is omitted, time is saved, application range of the oral preparation is widened, and curative effect is evident. The structural formula (I) is shown.
WO2014041885A1 Cholecystokinin secretion-promoting composition A novel CCK secretion-promoting substance and a use thereof are provided. This cholecystokinin secretion-promoting composition contains, as an active component, an unsaturated aldehyde having a main chain of 4-12 carbon atoms having a double bond in at least position 2 or 4 and/or an acrylic acid, wherein the main chain has 4-9 carbon atoms if there is a double bond only in position 2 and the main chain has 9-12 carbon atoms if there is a double bond only in position 4. This cholecystokinin secretion-promoting composition can be used as an appetite suppressant. By adding this cholecystokinin secretion-promoting composition to food, appetite-suppressing food products can be provided.
WO2009094456A3 Use of high-dose, post-transplantation oxazaphosphorine drugs for reduction of transplant rejection A lymphocytotoxic, but hematopoietic stem cell-sparing, high-dose amount of an oxazaphosphorine drug such as, for example, cyclophosphamide, administered post-transplantation can be used to reduce transplant rejection, including graft-versus-host- disease (GVHD). In some embodiments, the transplants are bone marrow transplants or hematopoietic stem cell transplants carried out for the treatment of hematologic disorders, including hematologic malignancies and non-malignant hematologic disorders. In some embodiments, the transplants are carried for the treatment of hereditary hemoglobinopathies, such as sickle cell anemia and thalassemia.
US20110152382 Composition of molecular elements for phosphorylase kinase inhibition Symmetrical curcuminoids molecular compounds that have been found to have anti-injury activity. It has been shown to benefit burns, injured and inflamed skin and mucous membrane and photodamaged skin. The improvement is mediated via inhibition of phosphorylase kinase activity. Phosphorylase kinase is released within 5 minutes following injury. Blocking the elevated phosphorylase kinase activity released after injury by phosphorylase kinase inhibitors, such as symmetrical curcuminoids, results in rapid reversal of burns, skin and mucous membrane injury and inflammation, repair of photodamaged skin, and prevention of scar tissue formation after injury.
US7786106 such as 3-[(4-methoxybenzoyl)-amino]-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}phenyl beta -D-glucopyranoside, used as an activated blood coagulation factor X inhibitor; anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4′-bromo-2′-[(5-chloro-2-pyridyl) carbamoyl]-6′-β-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2′-(2-acetamido-2-deoxy-β-D-glucopyranosyloxy)-4′-bromo-6′-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.
US20100280089 Use of inhibitors of jun n-terminal kinases for the treatment of glaucomatous retinopathy and ocular diseases Compositions and methods for the treatment of glaucoma and other ocular diseases are disclosed. The compositions and methods are particularly directed to the use inhibitors of Jun N-terminal kinases (JNK), such as SP600125 in the treatment of glaucoma and other ocular diseases.
CA2659276A1 2-amido-4-isoxazolyl thiazole compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof 2-Amido-4-isoxazolyl thiazole compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.
CN201375684Y Simvastatin and nicotinic-acid double release capsule The utility model relates to a simvastatin and nicotinic-acid sustained-release capsule preparation, which comprises a capsule casing and medicinal preparations stuffed in the capsule casing, wherein the medicinal preparations are a simvastatin rapid-release tablet and a nicotinic-acid sustained-release tablet. The utility model has the advantages that the preparation process of the medicinal preparations is simple, thereby dispensing with the two steps of tablet compressing and achieving high finished tablet ratio as well as better synergistic release effect when the tablets are released in the body; and in the quality inspection of finished products, the capsule has better accuracy than a bilayer tablet while the two tablets are not interfered with each other.
CN103041192A Bedsore paste A bedsore paste comprises the following raw material medicines in terms of weight: 10 g of root of oriental buckthorn, 10 g of gastrodia elata, 10 g of rhizoma acori graminei, 10 g of fructus psoraleae, 10 g of metronidazole, 10 g of alums, 10 g of earthworm, 10 g of angelica sinensis, 10 g of white wax, 10 g of dragon's blood, 10 g of rhizoma coptidis, 10 g of pearl powder, 10 g of borneol, 10 g of achyranthes bidentata, 10 g of clusiaceae, 10 g of radix salicis babylonicae, 10 g of polygonum cuspidatum, 10 g of carbonized hair, 10 g of apiary, 10 g of musk and 10 g of fructus gleditsiae abnormalis. The bedsore paste provided by the invention has the advantages of good sore healing and myogenic effects and quick action.
WO2012055945A1 Indole derivatives and process for their preparation Substituted indole derivatives of formula (I) wherein the radicals have e. g. the following meaning: R1 is hydrogen, -C1-6-alkyl, R2 is hydrogen, -C1-6-alkyl or cycloC3-12-alkyl; R3 is OR R4 is hydrogen or halogen, R5 is hydrogen, -C1-6-alkyl R6 is hydrogen, -C1-6-alkyl R is hydrogen or -C1-6-alkyl; X is a group -C(O)CH2- or -CH=CH-; R7 is hydrogen are potent inhibitors of Abeta peptide polymerization and can be used for the treatment of e.g. Alzheimers disease or ocular disorders.
US20080188538 Administering rampiril; dysglycemia, where the patient has no history of cardiovascular disease The present invention is directed to methods of lowering glucose levels in a patient. More specifically, the present invention is directed toward methods of lowering glucose levels comprising administering a therapeutically effective amount of ramipril to a patient in need thereof.
US8232274 Pyridazinone derivatives useful as glucan synthase inhibitors Disclosed is a set of compounds useful as glucan synthase inhibitors having the generic structure of Formula I: wherein the various moieties A, D, R6, etc., are as defined in the specification. These compounds are useful in treating or preventing fungal infections in a patient.
US20080003254 Systems and methods for delivering a rapamycin analog that do not inhibit human coronary artery endothelial cell migration A drug-eluting endoprosthesis is configured for inhibiting restenosis and thrombosis, and for promoting healing of a lesion in a body of a subject. Such an endoprosthesis includes at least a supporting structure and a therapeutically effective amount of the rapamycin analog is disposed thereon. The therapeutically effective amount of the rapamycin analog allows for the rapamycin analog to elute from the supporting structure so as to obtain a concentration of the rapamycin analog that is sufficient for inhibiting restenosis and/or inhibiting thrombosis. Also, the therapeutically effective amount of rapamycin analog is substantially devoid of inhibiting cell migration such that migrating cells promote healing of the lesion.
CN103142946A Health-care medicine for expelling lead in human body The invention provides a health-care medicine for expelling lead in human body, belonging to the technical field of health product processing. The medicine is mainly used for helping human body to expel noxious material such as mercury element out of the body. The medicine comprises ginger essential oil, vitamin E, garlic extract, lactic acid zinc and licorice extract. The medicine releases active substances after entering the human body, and the active substances directly react with the mercury element to form a complex with can be expelled with urine or night soil. The medicine is good in lead expelling effect, nontoxic and harmless, and finally achieves effects of human body health care.
CN103385928A Compound medical preparation for curing diarrhea of young livestock and applications thereof The invention relates to a compound medical preparation for curing diarrhea of young livestock and applications thereof, and belongs to the technology field of medical preparation for livestock. In order to solve the problems of high cost, bad curative effect and slow effect in the prior art, the invention provides a compound medical preparation for curing diarrhea of young livestock. The compound medical preparation is mainly composed of following medicines in parts by weight: 6.0 to 12 parts of gentamycin sulfate(GEN), 15 to 30 parts of rhizoma corydalis, 15 to 20 parts of yeast powder and 15 to 30 parts of alum. The compound medical preparation has the advantages of low cost, good curative effect on young livestock and high cure rate. Furthermore, the components are used together to have a synergistic effect, and has the functions of invigorating stomach, regulating flow of Qi, disinfecting, diminishing inflammation, astringing to arrest diarrhea, relieving pains and stopping bleeding.
WO2009000150A1 The use of sanchinoside in treating septicemia The use of sanchinoside in treating septicemia, especially the use of Panax notoginsenosides in treating and/or preventing septicemia is provided in the prevent invention.
CN103755695A Amide compounds with antitumor activity and application of amide compounds The invention belongs to the technical field of medicines and particularly relates to amide compounds with antitumor activity and an application of the amide compounds. The amide compounds are as shown in the general formula (I), wherein R1 and R2 can be same or different and are respectively and independently selected from hydrogen, halogen, a cyan, hydroxyl, halogenated alkyl, alkoxy, alkoxylalkyl, alkylamino or alkylaminoalkyl; R3 is triazole, 1, 3, 4-oxa-diazole, carbonyl and respective corresponding electro-withdrawing or electron donating substituent groups; and X is carbon or nitrogen atoms. A pharmacological activity result of the amide compounds provided by the invention shows that the amide compounds have favorable inhibiting effect for tumor cell strains.
CN1814299A Macrolide antibiotics sodium hyaluronate eye transfer system This invention relates to an eye use transmission system of macrolide type antibiotic hyaluronic acid natrium. The goal of this invention is to provide a macrolide type antibiotic eye use medicine preparation with carrier is hyaluronic acid or its salt. It is used to cure germ eye region infection. The macrolide type antibiotic in this invention includes antibiotic that has 14 yuan,15yuan, 16yuan large ring construction features , for example, natural antibiotic bring by streptomycete erythromycin, josamycin, spiramycin, medemycin etc. and semisynthesis derivant from by structure modification of natural antibiotic, such as roxithromycin, azithromycin, clarithromycin, rokitamycin, telithromycin.
US20120004311 Optically pure apogossypol derivative as pan-active inhibitor of anti-apoptotic b-cell lymphoma/leukemia-2 (bcl-2) A compound of Formula I: or a pharmaceutically acceptable salt thereof is disclosed. In addition, pharmaceutical compositions thereof, methods for preparing and methods for using this compound or composition for treating a variety of diseases, including cancer and inflammation are also provided.
WO2008052432A1 A medicament for improving the semen quality and treating male infertility A medicament for improving the semen quality and treating male infertility. The medicament is composed of levocarnitine, arginine, vitamin E, nucleotide, zinc gluconate, clomifene, selenium citrate and vitamin A acetate, and the ratio thereof is from 140: 140: 7: 7: 7: 3.5: 1: 1 to 80: 80: 4: 4: 4: 2: 1: 1. The preparation method of said medicament comprises the steps of: (1) mixing the components of the medicament in the ratio uniformly, (2) adding excipients and mixing again, (3) drying and formulating into oral preparation. The components of the medicament have synergistic effect.
CA2724897A1 Salts and polymorphs of a tetracycline compound Crystalline forms, including salts and polymorphs, of a compound useful in the treatment of tetracycline compound-responsive states are provided herein. The crystalline compounds are useful for the treatment or prevention of conditions and disorders such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds in general.
US7001909 For therapy of cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes, and for increasing HDL plasma levels in mammals.
US20100152193 Pyridazinones The present invention is concerned with novel pyridazinones of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of CNS disorders.
US20080171727 Administering a photosensitive, non-antibiotic tetracycline, preferably chosen from CMT-1 through CMT-10, without administering a bisphosphonate compound; side effect reduction A method of treating acne in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat acne but has substantially no antibiotic activity, without administering a bisphosphonate compound.
WO2007074346A3 Modulation of wnt signalling pathways for treating nervous system disorders The present invention provides the use of a modulator of a Wnt signalling pathway in the preparation of a medicament for treatment of degenerative diseases or disorders where synaptic loss or afferent tone in central and peripheral nervous system is affected, such as Alzheimer's disease Amylotropic Lateral Sclerosis (ALS) and cerebral palsies.
US8575138 Method for providing neuroprotection A method for providing neuroprotection to a patient in need of neuroprotection, comprising administering a neuroprotective-effective amount of a compound of formula I in which X is an oxygen atom or an ═N—OH group, R is selected from the group consisting of A is a hydrogen atom or together with B a carbon-carbon bond, B is a hydrogen atom, a hydroxy group or together with A a carbon-carbon bond, C is a hydrogen atom or together with D a carbon-carbon bond, D is a hydrogen atom or together with C a carbon-carbon bond, E is a hydrogen atom or together with F a carbon-carbon bond, F is a hydrogen atom or together with E a carbon-carbon bond, or an addition salt with a pharmaceutically acceptable acid.
US20090117168 Device and method for attaracting diseased cells and foreign substances An implantable device for attracting diseased cells or foreign substances circulating within bodily fluid channels is disclosed. The device comprises a frame, an attachment means for maintaining the frame in a localized position in a body vessel, and at least one attractant on the frame, where the attractant is capable of attracting a diseased cell or a foreign substance. The device may also include a therapeutic agent The device may be used for diagnosis, disease containment or treatment. The device may also be used for attracting and localized treatment of diseased cells and foreign substances.
WO2010109212A3 Carrier comprising a vitamin e derivative A pharmaceutical composition is provided comprising a vitamin E derivative, an anionic phopholipid-binding protein, an anionic phospholipid and a sterol. Also provided is a method for preparing a composition for delivering a cargo to a subject comprising a) forming liposomes from a vitamin E derivative, an anionic phospholipid-binding protein such as annexin, an anionic phospholipid such as phosphatidylserine and a sterol; and b) encapsulating the cargo in the liposomal composition.
CA2232325C Tumor rejection antigens presented by hla-b44 molecules, and uses thereof Tumor rejection antigens presented by HLA-B44 molecules are described. These peptides are useful in diagnostic and therapeutic methodologies. The tumor rejection antigens are not derived from tyrosinase, which has previously been identified as a tumor rejection antigen precursor processed to an antigen presented by HLA-B44.
US20090252685 High penetration prodrug compositions of prostaglandins and related compounds The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
CN102898402A Benzisoselenazolone-modified pyrrolyl formate-substituted indolone compound and use thereof The invention discloses a benzisoselenazolone-modified pyrrolyl formate-substituted indolone compound and a use thereof. The invention depends on and claims the priority of a Chinese patent application 201110105248.0 submitted on April 26, 2011. Through reference, all contents of the Chinese patent application 201110105248.0 are incorporated into the invention. The benzisoselenazolone-modified pyrrolyl formate-substituted indolone compound is shown in the general formula I. The 2-indolone compound provided by the invention has excellent antitumor activity and can be widely used for preparation of antitumor drugs.
EP1718632A1 Pyrimidine derivatives as orexin receptor antagonists The present invention relates to the orexin receptor antagonists of the general formula (I), which are selective to orexin I receptors. (I) -wherein Ar stands for phenyl group or a 5- or 6-membered heterocyclic ring containing 1-3 identical or different heteroatoms or methylenedioxyphenyl group -these groups may optionally be substituted with one or more identical or different C1.4 alkyl group, halogen atom, hydroxyl group, C1-4 alkoxy group, trihalogenomethyl group, NHC1.4 alkyl, -N(CI-4 alkyl)2 or -NHC(=0)-C1-4 alkyl group,
CA2386810C Electrospun skin masks and uses thereof A skin mask for affecting a skin condition comprises a fibrous membrane comprising one or more fibers that have been electrostatically spun and applied directly onto the three-dimensional topography of the skin to form the membrane. The skin covering or mask contains one or more polymers and, optionally, one or more preferably medically useful additives for protecting and/or healing the skin. The skin mask is generated on the skin by directly electrospinning one or more polymeric fibers onto the skin surface.
US6852715 Formula (1) wherein R1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and R2 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon The invention provides compounds of formula (1) wherein R1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and R2 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof. The invention also relates to a process for obtaining the compounds, compositions containing them and their therapeutic use. The compounds display excellent activity against mammalian cancer cell lines.
EP1047423B1 Novel apoptosis inhibitors An apoptosis inhibitor which comprises a compound of formula (1) wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: -CO-, -CH(OH)- or -NR3- where R3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.
US20100168176 Novel compounds, pharmaceutical compositions containing same, and methods of use for same Compounds having the following general formula, pharmaceutical compositions comprising the compounds, and methods of treating cancer, obesity, and microbial infections using such compositions: wherein: R1=H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, cyanomethyl, —OCH3, OC(O)CH3 or OC(O)CF3 R2=-OCH2C(O)NHNH—R5, where R5 is (a) phenyl, optionally substituted with one or more of halogen, C1-C8 alkyl, optionally substituted with halogen, —OH, —OR6, where R6 is C1-C8 alkyl, optionally substituted with halogen, or (b) 2-, 3-, or 4-pyridyl, optionally substituted with halogen, —OH, —OR6, where R6 is C1-C8 alkyl, optionally substituted with halogen, or (c) a heterocycle selected from the group consisting of imidazole, thiazole, benzimidazole, benzoxazole, benzthiazole, tetrazole, triazole, and aminothiazole; or (d) —C(O)R7, where R7 is a C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, or a heterocycle selected from the group consisting of pyridyl, imidazole, thiazole, benzimidizole, benzoxazole, benzthiazole, tetrazole, triazole, and aminothiazole; and R3 and R4, the same or different from each other, are C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl.
WO2014039595A1 Imidazopyridazine jak3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
WO2008006626A1 Triphenyl modified 5-membered heterocycles and their use as anticancer and antiinflammatory agents The present invention provides 5-membered heterooycles, preferably pyrrole furans and thiophenes, with three phenyl moieties wherein at least one of the three Phenyl moieties is substituted with halogen and alkoxy, halogen and hydrox trihalomethy, and alkoxy, trihatomethyl and hydroxy or halogen and alky, an wherein a second phenyl moiety is substituted with at least hydroxy or alkoxy The compounds of the invention show antiproliferative effects and inhibitory effects on cyclooxygenases (COX-1 and COX-2). Therefore the invention is also directed to the use of said compounds for the manufacture of a pharmaceutic composition for prevention and treatment of cancer and/or inflammatory diseases The invention further concerns a method for treating cancer or an inflammator disease, which comprises the step of administering to a patient suffering from that disease a therapeutically effective amount of at least one of said compounds.
WO2005058306A1 Glutamine-containing energy imparting amino acid composition or amino acid solution [PROBLEMS] To provide an amino acid composition that can not only carry out efficient energy supplementation but also attain motor function enhancement, having substantially no side effects. [MEANS FOR SOLVING PROBLEMS] There is provided a glutamine-containing energy imparting amino acid composition or amino acid solution, characterized by comprising proline, alanine, valine, isoleucine, lysine and glutamine. This amino acid composition is superior in the above energy supplementation and motor function to the conventional amino acid compositions not containing glutamine.
US20080008662 Aerosol Drug Inhibition of Lung Cancer The present invention provides a method of inhibiting growth of lung metastases in an individual comprising the steps of administering a dose of a lipid-drug enhancer liposomal complex and, in sequence, administering a dose of a lipid-anticancer drug liposomal complex. Furthermore, the lipid-drug enhancer liposomal complex may be administered in a continuing dose with the lipid-anticancer drug liposomal complex whereby both liposomal complexes are mixed in the nebulizer. Methods of inhibiting growth of lung metastases in an individual by the sequential administration via aerosolization of a dilauroylphosphatidylcholine-cyclosporin A liposomal complex and a dilauroylphosphatidylcholine-paclitaxel liposomal complex are also provided.
CN103638515A Anti gram-positive bacterium composition of anglerfish skin collagen peptide The invention discloses an anti gram-positive bacterium composition of anglerfish skin collagen peptide, and the anti gram-positive bacterium composition is prepared by compounding an anglerfish skin collagen peptide solution with a concentration of 100-200 mg/ml and a ceftiofur sodium solution with a concentration of 20 mug/mL according to a volume ratio of 3- 4:1. By combination use and collaborative effects of anglerfish skin collagen peptide and antibiotic ceftiofur sodium, the anti gram-positive bacterium composition has a better bacteria resistance and bacteriostasis activity on gram-positive bacterium, reduces the antibiotic dose, reduces drug residues, avoids or reduces the production of drug resistant strains, and improves the economic added value of anglerfish skin.
CN102379873A Acute general Parkinson's disease monkey model and medicament screening method thereof The invention provides a preparation method for an acute general Parkinson's disease monkey model. The preparation method comprises the following step of: continuously applying 0.36 mg/kg of MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) to a monkey for five times once every two days in an intravenous injection way. The invention provides a method for screening a medicament for treating the acute Parkinson's disease. By performing continuous peripheral vein injection of MPTP, an acute general Parkinson's disease monkey model with symptoms similar to those of an advanced-stage Parkinson's disease patient can be established. The model has stable symptoms within 1-4 months after establishment, and recovers rapidly later.
WO2009023207A1 Thiazolium compounds for treating gastrointestinal complications The present invention relates to a method of treating gastrointestinal complications e.g., complications related to a reduction of nNOS expression, and more particularly gastroparesis and diabetic enteropathy, using thiazolium derivatives.
US20090069286 Deuterium-enriched aztreonam The present application describes deuterium-enriched aztreonam, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2014110154A1 Methods and comp0stions for treatment of demyelinating diseases Disclosed herein are new oral pharmaceutical compositions of SAMDC inhibitors, polyamine analogs, and polyamine biosynthesis inhibitors, and their application for the treatment of conditions including demyelinating diseases, autoimmune disorders affecting the nervous system, and other neurodegenerative conditions.
WO2007018234A1 Agent for increasing urethral pressure It is intended to provide a novel agent for increasing urethral pressure. The invention relates to the agent for increasing urethral pressure containing tramadol or a pharmaceutically acceptable salt thereof as an active ingredient or a therapeutic agent or a preventive agent for stress urinary incontinence.
WO2005115547A2 Myricitrin compounds for sleeping disorders Provided herein is a composition that contains an effective amount of one or more compounds in particular myricitrin and related compounds for treating, preventing, or ameliorating a disorder such as insomnia or another sleeping disorder and using the composition.
CN1861052A Slow-releasing injection contg. platinum compound and cytotoxin type anticarcinogen A slow-release anticancer injection contains the slow-release microspheres and solvent. Said slow-release microsphere contains the active anticancer component chosen from 6 Pt compounds including bicycloplatinum, etc and 4 cytotoxins including taxane, alkylating agent, topologic enzyme inhibitor, or plant alkaloid, and the slow-release auxiliary.
CN101766642A Application of panaxoside Rd in preparing medicament for preventing and curing Alzheimer's disease The invention relates to application of panaxoside Rd in preparing medicament for preventing and curing Alzheimer's disease. Experiments show that the injury of nerve cells in the Alzheimer's disease can be simulated by three-dimensionally and directionally injecting beta amyloid to bilateral sea horse CA1 areas, the toxicity effect of A beta on the nerve cells can be remarkably relieved by providing the panaxoside Rd in advance, the number and form of propagated and activated astrocytes are recovered to be normal, the ultra microstructures of the abnormal cells in the CA1 areas are improved, the expression of caspase-3 can be obviously reduced, and the panaxoside Rd has obvious protection effect on the injury of the nerve cells in the Alzheimer's disease.
CN102964384A Adefovir dipivoxil gallic acid eutectic, and preparation method and composition thereof The invention discloses adefovir dipivoxil gallic acid eutectic, and a preparation method and a composition thereof. The eutectic is combined by adefovir dipivoxil, gallic acid and water according to molar ratio of 1:1:1. The crystal form of the adefovir dipivoxil gallic acid eutectic disclosed by the invention is stable and is unlikely to decompose if being stored under common conditions, is high in the bioavailability, and is liable to prepare. The method is moderate in reaction conditions and is liable to control; and as shown in element analysis and DSC analysis results, the prepared adefovir dipivoxil gallic acid eutectic has high purity and low impurity content.
US7129366 an end-terminal group, which is isopropyl, sec.-butyl, or tert.-butyl group; a leading group; and a long-chain aliphatic, non-cyclic, saturated or unsaturated, hydrocarbon group that links end-terminal group and leading group; for cancer therapy, prevention, and immune boosting and inflammation functions Compounds containing a specific saturated or unsaturated branched chain terminal group; a polar leading group; and a long-chain aliphatic, non-cyclic, saturated or unsaturated, substituted or unsubstituted, hydrocarbon group linking them; and having anti-cancer, immunosuppression alleviation, immune boosting and anti-inflammation activity.
CN103638379A Rheumatism treatment plaster The present invention discloses a rheumatism treatment plaster, which comprises a paste body and all-cotton gauze, wherein the paste body is coated on the all-cotton gauze. The rheumatism treatment plaster is characterized in that the rheumatism treatment plaster comprises the following raw drug components, by weight: 45-50 parts of sesame oil, 10-15 parts of red lead, 3-5 parts of prepared common monkshood mother root, 2-4 parts of chuanlong yam rhizome, 3-4 parts of doubleteeth angelica root, 3-5 parts of ovientvine stem, 4-6 parts of rhmannia glutinosa, 3-4 parts of baikal skullcap root, 3-5 parts of raw coix seed, and 2-3 parts of pilose antler. The present invention further provides a method for preparing the plaster. According to the present invention, the plaster is prepared through combining the modern technical condition strictly according to the preparation method requirements based on the Chinese medical science syndrome differentiation treatment and the formula summarized for a plurality of years, is specially provided for treating rheumatism, and provides a significant effect, wherein the one plaster can be used multiple times, usually the plaster is replaced one time a week, the one treatment course time is a month, and the patient rheumatism is basically cured and no recurrence is generated after the three treatment courses.
US20120231078 Method to reduce the symptoms of heartburn and gastro-oesophageal reflux disease (gerd) by specific polysaccharides The invention is directed to the use of a specific group of polysaccharides for reducing the symptoms of heartburn and gastroesophageal reflux isease. In addition, a pharmaceutical preparation is provided comprising a specific group of polysaccharides having a high hydration rate, a high viscosity, and a high stability at low pH. Such a preparation is particularly effective in reducing the symptoms of heartburn and/or gastro-oesophageal reflux disease, particularly when consumed in dry form.
US20090232895 Procedure and devices for the controlled obtaining of dry saline aerosols with therapeutic effect The patent refers to a procedure and devices for the generation of dry aerosols, continuously, by mechanic self-erosion, by average stirring in air or air-oxygen feed, of some crystals with special structure obtained by controlled crystallization processes. There can be also used other salts known to have physiological effects or mixtures of saline crystals with capacities close to the micro-particle generation. The devices can be for human or veterinary individual use, in intensive therapies or for producing aerosols with therapeutic or preventive effect in public rooms.
CN101676319A Medical sodium hyaluronate gel for injection The invention provides a medical sodium hyaluronate gel for injection, which can meet the treatment needs in the medical field, has no side-effect and good disinfection and storage stability. The medical sodium hyaluronate gel for injection containing citric acid or sodium citrate is added into a medical sodium hyaluronate gel aqueous solution.
CN101306194A Medicine for treating nerves damage and preparation method thereof The invention provides a medicine used for curing nerve damage and a method used for preparing the medicine. The invention belongs to the technical field of a biologic medicine. The medicine is prepared with snake venom nerve growth factors NGF, neurotrophy factors NTF, nerve stem cells and Schwann cells according to the following method: the entire spinal cord of a newborn animal or a fetus which can not be conceived because of natural and man-made calamities is implanted in aseptic PBS liquid or culture fluid; required ganglia are cleaned and shorn again and again. After the required ganglia are cultured in a thermostat of 37 DEG C for 48 hours, little culture fluid is added; the required ganglia are cultured for eight days before the required ganglia are frozen and deposited for passage. Before operation, the frozen and deposited cells are revived, and are implanted in the pia mater spinalis of the damaged spinal cord. The medicine can provide the cultured cells and the damaged neurocyte with new nutriments and NGF required for promoting the growth. The implanted cells can be separated and added to the damaged neural parts to repair the damaged, dead or feeble cells with safe and remarkable cure effect.
US7521479 Administering chaotropic agent The invention is related to the treatment of prion-related diseases such as the transmissible spongiform encephalopathies (TSEs) in mammals by administering chaotropic agents to or inducing a hyperthermia state in the affected mammals.
CN102512519A Medicinal moxa roll for treating osteoporosis and preparation method thereof The invention discloses a medicinal moxa roll for treating osteoporosis and a preparation method thereof. The medicinal moxa roll is prepared from the following bulk pharmaceuticals by weight: 26-40g of moxa punk, 0.67-1g of divaricate saposhnikovia root, 0.67-1g of large-leaved gentian, 0.67-1g of notopterygium root, 0.2-1.2g of rhizoma corydalis, 0.8-1.2g of tree peony root-bark, 0.67-1g of double-teeth pubescent angelica root, 0.8-1.2g of himalayan teasel root, 0.8-1.2g of pawpaw, 0.8-1.2g of Chinese atractylodes, 0.8-1.2g of red paeony root, 1.07-1.6g of realgar and 0.5-0.5g of moschus. The medicinal moxa roll has the advantages of good treatment effect on osteoporosis, no toxic or side effect, safety, no pain and low treatment cost.
US20110293715 Pharmaceutical Formulation and Process for Its Preparation The present invention relates to a multiparticulate tablet with improved gastro-protection comprising at least a pharmaceutically active substance in the form of enteric coated particles, and a mixture of tableting excipients, wherein the said mixture of excipients comprising xylitol and/or maltitol, each in a directly compressible form, a disintegrating agent, a lubricant and at least one other diluent and the ratio of a) the xylitol and/or the maltitol to b) the other diluent(s) is less than 5/95 (weight/weight) and the result of the “test of integrity of the film” is greater than 95%, preferably greater than 97% and more preferably still greater than 99% and the result of the “release test” is greater than 90%, preferably greater than 95%. According to one embodiment of the invention, the active substance is omeprazole or esomeprazole. According to another embodiment the tablet is a disintegratable tablet, which disintegrate in the mouth with or without chewing. The invention also comprises a process for preparing the claim tablet and its use in medicine.
WO2009063836A1 Process for production of polyphenol extract, prophylactic agent for osteoporosis, saccharide-digesting enzyme inhibitor, functional composition comprising the polyphenol extract, and food composition, food composition for specified health uses, quasi drug composition and pharmaceutical composition each comprising the functional composition Disclosed are: a method for producing a polyphenol extract which does not contain citric acid, which contains a polyphenol component having a definite composition, and which contains the polyphenol component in a large quantity; a functional composition, a prophylactic agent for osteoporosis and a saccharide-digesting enzyme inhibitor for the treatment or prevention of obesity or diabetes, each of which comprises the polyphenol extract; and a food composition, a food composition for specified health uses, a quasi drug composition and pharmaceutical composition. The method for producing a polyphenol extract comprises the steps of: contacting a plum vinegar with a styrene-divinyl benzene synthetic absorption resin; subjecting the styrene-divinyl benzene synthetic absorption resin to the elution treatment with an aqueous solvent; and concentrating the eluted solution, thereby producing a polyphenol extract which does not contain citric acid and contains a polyphenol component in a high concentration. A novel functional composition containing the polyphenol extract produced from a plum vinegar can be used as a food composition for preventing diabetes, a food composition for specified health uses, a quasi drug composition or a pharmaceutical composition.
US20080096891 Triazine derivatives, their preparation and therapeutic application thereof The invention relates to triazine derivatives of general formula (I): Wherein R1, R2 and R3 are as defined herein. The invention also relates to a method for preparing these triazine derivatives and to the therapeutic application thereof.
WO2012135669A1 Nitrogen ring containing compounds for treatment of inflammatory disorders The invention provides compounds, pharmaceutical compositions and methods of treatment of inflammatory disorders including a compound of Formula I, or its pharmaceutically acceptable salt, ester, pharmaceutically acceptable derivative or prodrug wherein R1, R2, R3, R4, X, Y, W, Z and Q are as defined herein.
WO2011044307A1 Phenyloxadiazole derivatives as pgds inhibitors This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
US20110034529 Benzene, pyridine, and pyridazine derivatives Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
US20110130392 Method of Administering a Methylene Blue - Curcumin Analog for the Treatment of Alzheimer's Disease A method of administering a methylene blue-curcumin hybrid useful in treating or preventing Alzheimer's Disease.
US7001611 Using astaxanthin; sleep disorders The present invention provides a circadian rhythm normalizing composition containing astaxanthin and/or its ester as an active ingredient, and a composition having the action of enhancing the circadian rhythm normalizing action of melatonin by protecting melatonin. The composition can be in the form of a drug, a functional food, a food or a beverage. This composition has a circadian rhythm normalizing action, and has the action of preventing or alleviating sleep disorder and various diseases due to disturbance of the circadian rhythm.
US7795204 supplementing the diet of an athlete with substances which increase the concentration of nitric oxide (NO) or increase its half life in the body, in combination with a source of amino acids, may provide surprising enhancement of an athlete's muscle Food supplement compositions and their methods of use in increasing lean mass and/or muscle size and/or strength in individuals, particularly, athletes is described. The food supplements described comprise a substance which increases nitric oxide production in the body, and, a source of amino acids. Other food supplements described comprise a substance which can enhance and/or mimic insulin activity, and a source of amino acids. The food supplement compositions described are suitable for supplementing the diet of an athlete and particularly for enhancing an athlete's muscle size or strength.
CN103393890A Drug for treatment of heat strangury The invention provides a drug for treatment of heat strangury, and the drug includes the following components: by weight, 8-12 parts of plantain seed, 6-14 parts of talcum, 5-15 parts of polygonum aviculare, 8-14 parts of cortex phellodendri, 6-12 parts of viola yedoensis, 5-10 parts of aquilaria wood, 8-12 parts of rheum officinale, 10-15 parts of yam rhizome, 7-14 parts of green tangerine peel, 8-12 parts of radix linderae, 8-11 parts of root of large-flowered skullcap, 6-12 parts of bupleurum and 8-12 parts of licorice. The drug has the advantages and positive effects of good curative effect, small side effect and low treatment cost.
CA2624025A1 Regimen of administration for 5-(2-chlorophenyl)-1 ,2-dihydro-7-fluoro-8-methoxy-3-methyl-pyrazolo [3, 4.-b] [1, 4] benzodiazepine The present invention relates to the use of the compound of the formula (I) for the manufacture of medicaments for the treatment of cancer, said medicaments being characterized by delivering the above compound in amounts of about 1.5 mg/m2/day to 5 about 30 mg/m2/day; as well as methods for treating cancer by administering said medicaments.
WO2012146890A1 Prebiotic agent A composition for the improvement of gastrointestinal health and/or for the improvement of a gastrointestinal bacterial population is provided. The composition comprises a prebiotic, is adapted for selective targeting of the prebiotic to the colon and is substantially free from probiotic.
US7683067 3-heterocyclyl-indole derivatives as inhibitors of glycogen synthase kinase-3 (GSK-3) Compounds of formula Ia or Ib wherein P; R1; R2; m; and n are as defined in the application, salts thereof, processed for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.
US20120142666 Azetidine 2-Carboxamide Derivatives Which Modulate The CB2 Receptor Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
US20070116784 Imatinib combinations for head and neck cancers 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of the formula I or a pharmaceutically acceptable salt thereof can be used in the treatment of head and neck cancers.
CN102885796A Lacosamide tablet for treating epilepsy and preparation method for lacosamide tablet The invention relates to a tablet for treating epilepsy and a preparation method for the tablet, in particular to a lacosamide tablet for treating epilepsy and a preparation method for the lacosamide tablet. The lacosamide tablet comprises lacosamide, an inclusion material, filler, disintegrant, lubricant and/or wetting agent, adhesive and a coating material. The main medicine lacosamide is coated by the inclusion material, and other auxiliary materials are added into the lacosamide, so that a tablet core is obtained, and a finished product is obtained after the tablet core is coated by the coating material. The obtained lacosamide tablet is relatively high in dissolution rate, medicine stability is greatly improved, and medicine-using risks are reduced.
US7902151 Methods and compositions for modulating immunity Methods and compositions for inducing immune suppression are disclosed. The methods involve administering an effective amount of a CD200 protein or a nucleic acid encoding a CD200 protein. The methods are useful in preventing graft rejection, fetal loss, autoimmune disease, and allergies. Methods and compositions for preventing immune suppression are also disclosed. The methods involve administering an effective amount of an agent that inhibits CD200. Such methods are useful in treating cancer.
WO2008107301A2 Rapid-disintegration monolayer film for the oral administration of active substances Rapid-disintegration monolayer film for the oral administration of active substances, comprising a water-soluble support containing at least one active substance, characterized in that it comprises a polymeric mixture of a hydrophilic film-forming agent formed from a copolymer of polyvinyl alcohol and of polyethylene glycol (PVA-PEG), of an active substance and of a hydrophilic gelling agent.
CN103462903A Combination method and preparation process of pioglitazone hydrochloride sustained-release pellet preparation The invention relates to a combination method and a preparation process of a pioglitazone hydrochloride sustained-release pellet preparation. The method comprises the following steps: mixing pioglitazone hydrochloride, a solubilizing agent and an adhesive uniformly; applying an medicine to a blank pellet core to prepare a pioglitazone hydrochloride medicine-containing pellet core; preheating the pioglitazone hydrochloride medicine-containing pellet core; and spraying sustained-release layer coating liquid onto the pioglitazone hydrochloride medicine-containing pellet core to prepare a pioglitazone hydrochloride sustained-release pellet. A compound metformin hydrochloride pioglitazone hydrochloride pellet preparation prepared by mixing the pioglitazone hydrochloride sustained-release pellet and a metformin hydrochloride sustained-release pellet achieves an ideal blood sugar reducing effect, can reduce toxic or side effects of the medicine, can reach a sustained and stable blood sugar reducing effect in a human body, is favorable for improving the compliance of patients, has high bioavailability and stable blood concentration, and can effectively improve the clinical curative effect, thereby providing a better dosage regimen and curative effect to diabetic patients at home and abroad.
CN102617462A Specificity inhibition muscle micro ribonucleic acid compound and synthesis method and application thereof Disclosed is a specificity inhibition muscle micro ribonucleic acid compound and a synthesis method and an application thereof, and the compound has the structure shown in following formula. The luciferase result and the real-time quantitative polymerase chain reaction (RT-qPCR) result both prove that the compound can inhibit muscle specificity micro ribonucleic acids.
WO2010128038A1 Hydroquinone derivatives Compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings given in the specification, are useful in the treatment of neurodegenerative disease.
WO2012145581A1 Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
CN101869612A Maxingshigan oral liquid and preparation method thereof The invention discloses maxingshigan oral liquid and a preparation method thereof. The preparation method comprises the following steps: taking 1000-2000 parts of gypsum and crushing into coarse powder; packing with gauze; decocting twice with 200-400 parts of ephedra, 200-400 parts of bitter apricot seed, 200-400 parts of liquorice, and 3000-6000 parts of water; merging the decocted liquid, filtering, concentrating the filter liquor to 500-1000 parts into dense paste, adding 200-400 parts of sucrose, 2-4 parts of benzoic acid, and 2-4 parts of ethylparaben, stirring, stewing, filtering to obtain 1000ml, and bulking to obtain the finished oral liquid. The preparation technology in the invention has simple control, high bioavailability, good and rapid curative effect and low cost.
CN102319203A Preparation method of levofloxacin lactate and sodium chloride injection The invention relates to a preparation method of a levofloxacin lactate and sodium chloride injection, and the method comprises the steps such as dense preparing, heating, filtering, diluted preparing, pH value regulating, filtering, filling, sealing, sterilizing, inspecting and the like. The levofloxacin lactate and sodium chloride injection prepared by the preparation method has good stability, and can completely be packaged by adopting a plastic bottle.
EP1791840A1 Substituted bicyclic imidazo-3-ylamine compounds The invention relates to substituted bicyclic imidazo-3-ylamine compounds of general formula (I), methods for production, medicaments containing the same and use thereof for the production of medicaments.
EP1562925B1 Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
US20110165221 Wound care A method for treating a wound, and a dressing for wound care management comprising a three-dimensional body of glass-based fibers comprising one or more glass-formers selected from the group consisting of P2O5, SiO2, and B2O3; at least about 25 wt % of the fibers have a diameter between about 200 nm and about 4000 nm, and a length:width aspect ratio of at least about 10. In another form, the glasses are in the form of particles in an ointment or cream applied to a wound. In yet other forms the glasses are employed as fibers formed into sutures for closing a wound, or as particles in a surgical glue for closing a wound.
CN101513409B Pharmaceutical composition of cephalexin The present invention discloses a pharmaceutical composition of cephalexin, which comprises cephalexin, adhesive, edulcorant and flavoring agent, wherein, the mass percentage of cephalexin is 10% -50%. The mass percentage of adhesive is 10%-50%. The mass percentage of edulcorant is 5%-90%. The invention adopts the essence with flavor masking function for masking the special flavor in the pharmaceutical composition of cephalexin and improves the mouthfeel of medicine particle through adding edulcorant. The invention researches out the contents of optimal flavor masking essence and edulcorant through large number of experiments. The medicine particle of cephalexin prepared according to the formula of the invention has the advantages of no bad smell in medicine taking, fragrant and sweet taste for facilitating the medicine taking of patient.
CN1754533A Tamoxifen citrate oral disintegrating tablet and its preparation method The invention discloses an oral disintegrating tablet of tamoxifen citrate, which comprises tamoxifen citrate, crumbling agent, drying and binding agent, bulking agent, flow aid, lubricating agent and sweetener. The preparing process comprises sieving, mixing homogeneously, and pelleting directly. The tablet can be disintegrated rapidly in mouth cavity without the presence of water.
CN101590021A Cefuroxime axetil odor-masking pellet and preparation method The invention relates to a cefuroxime axetil odor-masking pellet and a preparation method thereof. The cefuroxime axetil odor-masking pellet consists of an uncoated pellet containing the cefuroxime axetil and an odor-masking layer coating outside the uncoated pellet. The cefuroxime axetil odor-masking pellet overcomes the defect of bitter taste of the prior cefuroxime axetil tablets, and provides a novel cefuroxime axetil preparation which masks bitter taste, releases medicament rapidly and has stable quality.
EP1505962A2 Monotherapy for the treatment of parkinson's disease with cyclooxygenase-2 (cox 2) inhibitor(s) A method of treating, preventing, or inhibiting PD, in a subject in need of such treatment, inhibition or prevention. The method comprises treating the subject with one or more cyclooxygenase-2 selective inhibitor(s), ester(s), salt(s) or prodrug(s) thereof, wherein the amount of the cyclooxygenase-2 selective inhibitor(s), ester(s), salt(s) or prodrug(s) thereof constitutes a PD treatment, inhibition or prevention effective amount of the COX 2 inhibitor(s).
WO2014033077A1 Composition comprising an antibiotic and a beta-lactamase inhibitor, wherein at| least one of them is in the form of mini-tablets The present invention relates to a composition comprising a first granule with an antibiotic and a second granule with a β-lactamase inhibitor wherein at least one of the granules is a mini-tablet (a particle with defined dimensions), a composition contained in a sachet, pharmaceutical compositions comprising mini-tablets, the use of mini-tablets and a process for the preparation of mini-tablets.
CN101204532B Medicine for prostate disease and preparation method thereof The invention relates to a medicine for treating prostate and a preparation method thereof.The medicine for treating prostatitis of the invention is prepared by the following materials: 10g of tall gastrodis tuber, 10g of ginger pinellia, 5g of astragalus root, 3g of garden burnet root, 5g of psoralea root, 5g of purslane speedwell, 10g of jujube seed, 5g of dahurian angelica and 5g of actinolitum. The method of the invention for preparing the medicine used for treating the prostatitis comprises the following steps that: crude drug of tall gastrodis tuber, ginger pinellia, astragalus root, garden burnet root, psoralea root, purslane speedwell, jujube seed, dahurian angelica and actinolitum are scaled to be pulverized into powder; 50g of honey is boiled; the drug is poured into the boiled honey to be stirred evenly; pills are made by dividing weight.The invention has the advantages of dramatic healing efficacy of clinical application, distinguishing drug potency, good drug property, treatment of both manifestation and root cause of disease, security and reliability, oral taking without provocation to internal organs, widely application, economical and practical, wide medicinal herbresource, small side effect, little toxicity, convenient usage, easy to carry, manufacture, transport and store, as well as wide market prospect.
CN101812052B Quinoline carboxylic acid derivative containing isatin substitute and preparation method thereof The invention relates to a quinoline carboxylic acid derivative containing isatin substitute, a preparation method, medical purposes, and an anti-tuberculosis drug combination containing the quinoline carboxylic acid derivative. More specifically, the invention relates to a new fluoroquinolone carboxylic acid derivative. The 7-site of the derivative on a quinoline core is 3-[N- methyl-N-2-(beta-substitute imino isatin-1-radical) ethyl] amino-1- piperidyl, the 8-site is methoxy group, and the 1-site is cyclopropyl. Compared with the traditional clinical anti-tuberculosis drug of a fluoroquinolone class (such as Ciprofloxacin), the quinoline carboxylic acid derivative has more excellent anti-tuberculosis mycobacterium activity.
US7820792 isoform of the alpha 2 delta -4 subunit of a voltage gated calcium channel; useful to identify modulators of the channel subunit; for cancer and inflammation The present invention provides nucleic acid and polypeptide sequences describing an isoform of the α2δ-4 subunit of a voltage gated calcium channel. The nucleic acids described herein can be used to produce functional α2δ-4 protein. The calcium channel α2δ-4 protein may be isolated for the purposes of binding experiments or may be used in cells to form a functional calcium channel complex.
US7427618 e.g. 2-[3-(4-ethynylphenyl)ureido]-N-[4-(3-oxomorpholin-4-yl)phenyl]valeramide; anticoagulant, antitumor factor; thromboses, myocardial infarction, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty, claudicatio intermittens, or migraine Novel compounds of the formula (I), in which R1, R2, R3, X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.
CA2186892C Methods for treating pulmonary vasoconstriction and asthma This invention is a method for treating or preventing bronchoconstriction or reversible pulmonary vasoconstriction a mammal which method includes: a) causing the mammal to inhale a therapeutically effective amount of gaseous nitric oxide, and b) introducing into the mammal a therapeutically effective amount of phosphodiesterase inhibiting compound; and an inhaler device (10) containing nitric oxide gas, and a phosphodiesterase inhibiting compound (106).
US20090117107 Molecular targets and compounds, and methods to identify the same, useful in the treatment of bone and joint degenerative diseases The present invention relates to methods for identifying agents capable of inhibiting the expression or activity of proteins involved in the processes modulating osteoclastogenesis, which inhibition is useful in the prevention and/or treatment of bone and joint degenerative diseases and diseases involving aberrant activity or differentiation of osteoclasts. In particular, the present invention provides methods for identifying agents for use in the prevention and/or treatment of rheumatoid arthritis.
US20110178044 Transdermal administration of hydrophilic drugs using permeation enhancer composition Methods, formulations, and drug delivery systems are provided for enhancing the flux of a transdermally administered hydrophilic drug using a basic permeation enhancer composition. The enhancer composition contains an inorganic hydroxide and a weaker, nitrogenous base, wherein the bases are selected such that a 0.1M aqueous solution of the nitrogenous base has a pH that is about 1.0 to about 6.5 lower than the pH of a 0.1M aqueous solution of the inorganic hydroxide. Additionally, the molar ratio of the nitrogenous base to the inorganic hydroxide in the enhancer composition is in the range of about 0.5n:1 to about 20n:1, where n is the number of hydroxide ions per molecule of the inorganic hydroxide.
US20090156547 1-(2,2-Difluoro-2-deoxy-b-D-ribofuranosyl)-4-(2-propyl-1-oxopentyl)amino-pyrimidin-2-one p-toluenesulfonic acid co-crystal; delivery by mouth;bioavailability; nontoxic; side effect reduction; hydrolysis to gemcitabinewith reduction of the formation of deoxydifluorouridine The present invention relates to novel amide prodrugs of gemcitabine, compositions thereof and methods for using.
US7608615 Pyrrolo[2,1-C][1,4]benzodiazepine hybrids and a process for the preparation thereof The present invention provides quinazolinone linked pyrrolo[2,1-c][1,4]benzodiazepine hybrid of general formula 5, wherein, R is alkyl or halo group selected from H, Cl, F or CH3 and n=1 to 3 useful for antitumour/anticancer activity. The present invention also provides a process for the preparation of quinazolinone linked pyrrolo[2,1-c][1,4]benzodiazepine hybrid general formula 5.
EP2599473A1 Astaxanthin-containing aqueous composition, cosmetic preparation, and method for suppressing degradation of astaxanthin Disclosed are an aqueous cosmetic preparation including at least (A) astaxanthin, (B) 20 µg/L or more of iron ions, and (C) an iron chelating agent, and a method for suppressing the decomposition of astaxanthin in which (C) an iron chelating agent is included in an aqueous composition including at least (A) astaxanthin and (B) 20 µg/L or more of iron ions.
CN103550319A Outer application preparation for treating knee athletic injury and preparation method thereof The invention discloses an outer application preparation for treating knee athletic injury and a preparation method thereof. The outer application preparation is mainly prepared from the following raw materials in parts by weight: 2-5 parts of radix clematidis, 2-4 parts of kudzu root, 1-6 parts of manganese black, 2-5 parts of ground beetle and 1-2 parts of indico naturalis. The outer application preparation has an obvious effect on treating knee athletic injury; the combination of the medicines generates an synergetic effect of the medicines; and the outer application preparation has the effects of dredging collaterals, promoting tissue regeneration, removing blood stasis, connecting bones, alleviating pain and strengthening the bones and muscles, thereby effectively treating knee athletic injury. By adopting the locally common medicines, the outer application preparation is low in price and reduces the economic burden of the patient.
WO2005063704A1 Azetidine ring compounds and drugs comprising the same It is intended to provide compounds having EDG-5 antagonism. Because of having EDG-5 antagonism, compounds represented by the following general formula (I): (I) wherein each symbol is as defined in the description; salts thereof, N-oxide derivatives thereof, solvates of the same or prodrugs of the same are useful as preventives and/or remedies for EDG-5-mediated diseases for example, diseases caused by blood vessel contraction (for example, cerebrovascular spasms disease, cardiovascular spasms diseases, coronary artery spasms disease, hypertension, pulmonary hypertension, renal diseases, myocardial infarction, angina, arrhythmia, portal hypertension, varicosity, etc.), arteriosclerosis, pulmonary fibrosis, hepatic fibrosis, renal fibrosis, respiratory diseases (for example, bronchial asthma, chronic obstructive pulmonary disease, etc.), nephropathy, diabetes, hyperlipemia and so on.
CN1682754A Ginseng-gaboderma lucidum tranquilizing dripping pill and its preparing method The present invention relates to one medicine composition for treating deficiency of vital energy yin, insomnia and dreaminess, palpitation and hard breath, valetudinarianism, etc. and the medicine composition is prepared into rally taken preparation, especially tranquilizing dripping pill, with Coriolus Versicolor polysaccharide and ginseng stem and leaf saponin as active medicine components. The present invention has high bioavailability, fast medicine release, fast acting, high medicine component content and other advantages.
WO2013022280A2 N1-cyclic amine-n2-substituted biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same An N1-cyclic amine-N2-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
US20080188537 Method of treating bipolar depression with a benzamide derivative A benzamide derivative, especially amisulpride, is used to prevent or treat bipolar depression of a patient suffering from bipolar disorder I or bipolar disorder II.
EP2473490A1 (thio)morpholine derivatives as s1p modulators The present invention relates to (thio)morpholine derivatives of the formula (I), wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyloptionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms,amino, di(1-4C)alkylamino, -SO2-(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl, -NH-CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from -CO-O-, -O-CO-, -NH-CO-, -CO-NH, -C=C-, -CCH3-O- and the linking group –Y-(CH2)n-X- wherein Y is attached to R1 and selected from a bond, -O-, -S-, -SO-, -SO2-, -CH2-O-, -CO-, -O-CO-, -CO-O-, -CO-NH-, -NH-CO-, -C=C-and -C≡C-; n is an integer from 1 to 10; and X is attached to the phenylene / pyridyl group and selected from a bond, -O-, -S-, -SO-, -SO2 -, -NH, -CO-, -C=C-and -C≡C-; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R5 wherein the alkylene group may be substituted with (CH2)2 to form a cyclopropyl moiety or one or two halogen atoms, or R3 is is (3-6C)cycloalkylene-R5 or -CO-CH2-R5, wherein R5 is -OH, -PO3H2, -OPO3H2, -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R6 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is -O-, -S-, -SO- or -SO2-; or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
CN103550671A Application of Zhenlong refreshing pharmaceutical composition in preparation of medicine for treating diabetic peripheral neuropathy The invention discloses an application of a Zhenlong refreshing pharmaceutical composition in preparation of a medicine for treating diabetic peripheral neuropathy. A Zhenlong refreshing preparation is traditionally used for treating acute cerebral infarction, carotid atherosclerosis plaque, apoplexy sequela, etc. Pharmacological experiments and clinical observations prove that the Zhenlong refreshing pharmaceutical composition disclosed by the invention comprises a Zhenlong refreshing capsule and a Zhenlong refreshing pharmaceutical composition prepared by an improved process, the Zhenlong refreshing pharmaceutical composition obviously perfects the symptoms of a nervous system of a DNP (diabetic peripheral neuropathy) patient and can significantly improve the nerve conduction velocity and perfect a variety of biochemical indexes, so that the Zhenlong refreshing pharmaceutical composition can be used for treating and preventing DPN.
WO2007111321A1 Method of analyzing sulfated polysaccharide or sulfated oligosaccharide, pharmaceutical composition and drug containing sulfated polysaccharide or sulfated oligosaccharide, method of producing the pharmaceutical composition and the drug and method of treating, diagnosing, symptom-relieving and preventing disease It is intended to provide: an analytical method whereby the structure of a sulfated polysaccharide or a sulfated oligosaccharide can be highly sensitively analyzed; a pharmaceutical composition and a drug containing a sulfated polysaccharide or a sulfated oligosaccharide having an excellent biological activity; a method of producing a pharmaceutical composition and a drug containing a sulfated polysaccharide or a sulfated oligosaccharide; and a method of treating, diagnosing, symptom-relieving and preventing a disease. A sulfated polysaccharide or a sulfated oligosaccharide is enzymatically digested and the obtained product containing a monosaccharide, a disaccharide or a trisaccharide is analyzed by mass spectrometry. Thus, the structure of the sulfated polysaccharide or the sulfated oligosaccharide is analyzed and its qualities such as a biological activity are evaluated, which makes it possible to produce an excellent pharmaceutical composition or drug. The above-described pharmaceutical composition and drug have excellent biological activities, that have been found hereby, relating to the tumor metastasis inhibitory activity, dengue virus-infection inhibitory activity, growth factor-binding activity and so on of chondroitin sulfate.
WO2006132583A1 Method and means for preventing and inhibiting respiratory disease, atherosclerosis and osteoporosis caused by chlamydia pneumoniae infection A method of treating respiratory infection, atherosclerosis, and osteoporosis in a patient caused by infection of Gram-negative bacteria having a Type III secretion, in particular by Chlamydia pneumoniae, comprises the administration of a pharmaceutical composition comprising a pharmacologically effective amount of a Type III secretion blocker and a pharmaceutically acceptable carrier. Also disclosed is a method for the manufacture of a medicament for use in said method of treatment.
CN1823779A Ruishufatatinggan soft capsule and its preparation method A soft capsule of Ruishufatadine calcium is prepared from Ruishufatadine calcium, diluent, cosolvent, suspending aid, surfactant and crystallizing inhibitor through mixing.
CN102038842A Medicament for improving production performance of pigs and preparation method thereof The invention relates to a medicament for improving production performance of pigs and a preparation method thereof. The medicament comprises the following components in percentage by weight: 15-25% of carvacrol, 10-15% of anise oil, 10-15% of tangerine peel oil, 6-10% of garlic essential oil, 5-7% of cinnamic aldehyde, 3-5% of thymol and 23-51% of white carbon black. The medicament provided by the invention is convenient to use, can be directly added to animal feed without toxic/side effects or medicament residues, and conforms to the requirements of the safe veterinary medicaments as well as the requirements for ensuring the safety of animal-derived food. The invention can enhance the palatability of feed, make pigs happier, improve the intestinal mucosa function, increase the digestibility, obviously promote the growth, improve the immunity, reduce the stress reaction, decrease the sickness rate of pigs and greatly improve the quality of meat.
CN102018593B Healing stone pillow for treating cervical spondylosis The present invention relates to a healing stone pillow for treating cervical spondylosis. The healing stone pillow of the present invention comprises healing stone pillow content and an overcoat fabric wrapped at outside of the healing stone content; the healing stone content comprises 55-75 parts by weight of opals, 25-45 parts by weight of stone needles and 0-20 parts by weight of conventionalpillow core fillers, preferably 60-70 parts by weight of opals and 30-40 parts by weight of stone needles. Medical stones and stone needles used by the present invention are natural mineral rocks which contain abundant macroelements and microelements needed by human body and can release infrared rays and ultrasonic radiations, so that good treatment and health care effects are provided to human bodies. In the present invention, medical stones and stone needles are mixed according to a certain proportion to be the contents of the healing stone pillow; after the two stones are heated, drug effects are released doubly; the healing stone pillow acts on focuses directly, has the functions of activating blood and dissolving stasis, reducing bloatedness and relieving pain, and specifically has good healing effect for cervical spondylosis. The present invention is simply structured, conveniently used and easily popularized.
CN102643220A Compound extracted from antrodia cinnamomea mycelium, and usage thereof The invention relates to a compound derived from antrodia cinnamomea mycelium. The invention also relates to a composition for treating or preventing hepatitis c virus (HCV) infection.
WO2013153161A3 Polymorph of rilpivirine hydrochloride The present invention relates to a novel polymorph and to novel solvates of rilpivirine hydrochloride, as well as to their preparation. The novel solvates are valuable intermediates for the preparation of the novel polymorph of rilpivirine hydrochloride of the present invention. Moreover the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and to methods of preparing the same. Finally the present invention relates to pharmaceutical combinations comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and additional therapeutic agents.
US20090012012 Intratracheal administration of endothelin-suppressing agents for the treatment of respiratory disorders The subject invention is directed to the treatment of respiratory disorders by intratracheal administration of an effective amount of an agent that suppresses the activity of endothelin. Such agents may take the form of: 1) an endothelin-converting enzyme (ECE) inhibitor such as phosphoramidon, or 2) an endothelin receptor antagonist such as bosentan, tezosentan, sitaxsentan, atrasentan, darusentan, clazosentan, or BQ-123. Respiratory disorders include emphysema, asthma, bronchitis, bronchiectasis, pneumonia, adult respiratory distress syndrome, neonatal respiratory distress syndrome, bronchopulmonary dysplasia, interstitial fibrosis, cystic fibrosis, persistent pulmonary hypertension of the newborn, and neoplasia. The treatment is intended for a variety of mammals, such as premature neonates to adult humans.
EP2190820A2 Substituted azepine- and diazepine-sulfonamides useful to inhibit 11beta-hydroxysteroid dehydrogenase type-1 In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11BETA-hydroxysteroid dehydrogenase type-1, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11BETA-hydroxysteroid dehydrogenase type-1 using such compounds or pharmaceutical compositions.
US20130028943 Melatonin tablet and methods of preparation and use The present invention provides a pharmaceutical composition for sublingual or buccal administration of actives with low to poor aqueous solubility, e.g. the indole hormone melatonin, which contains a solution of the active in a pharmaceutically acceptable solvent adsorbed or absorbed onto particles of a pharmaceutically acceptable carrier and methods of preparing and using the pharmaceutical composition.
CN101288641B Coenzyme Q10 water dispersion and preparation method thereof The invention relates to a coenzyme Q10 water dispersion and a preparation method thereof, which is composed of coenzyme Q10, pectin substances, emulsifier, polyethylene glycol or poloxamer and other excipients which are all edible, the hot-melt mixture of the coenzyme Q10 and the polyethylene glycol or the poloxamer is further mixed with the mixture of the pectin substances, sugar, the emulsifier and soluble starch, the heating and the heat preservation are carried out, after that, a colloidal mill and a high-pressure homogenizer or a high-speed shear emulsion mixer are used for homogenizing to prepare an even colloid; and the coenzyme Q10 water dispersion is finally prepared by spray drying. The coenzyme Q10 water dispersion and the preparation method are characterized in that the bioavailability is high, all the used excipients are edible, the safety is good, the whole preparation process does not use any organic solvent or antioxidant, thereby having no pollution on the product and the environment caused by the organic solvents, having small production difficulty and being applicable to the industrial production.
EP1712231A2 Method for improving the pharmacokinetics of tipranavir The present invention relates to a novel method for improving the pharmacokinetics of tipranavir, comprising administering to a human in need of such treatment a combination of a therapeutically effective amount of tipranavir or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of ritonavir or a pharmaceutically acceptable salt thereof.
EP0885228B1 Meso-substituted tripyrrane compounds, compositions, and methods for making and using the same A compound of formula (I) wherein: Q represents identical alkyl groups, cycloalkyl groups having from 5 to 7 ring atoms, or aryl or heteroaryl groups having from 5 to 12 ring atoms and R represents identical hydrogen, alkyl, alcohol or carbonyl-containing groups; or a composition containing from 5 to 100 mole % by weight of the compound of formula (I). A novel method for synthesizing the compounds of formula (I) comprises the steps of: (a) reacting a compound of the formula: Q-CHO or Q-CH(OS)(OS') wherein Q is as defined above and S and S' are independently lower alkyl, an aryl group containing from 5 to 14 ring atoms, and -(CH2)n- where n=2-4, with an excess amount of a pyrrole in the presence of a catalytic amount of a strong Lewis or Bronsted acid; (b) removing any unreacted pyrrole or other solvents used by evaporation; (c) removing polymeric materials and removing the corresponding dipyrromethane by-product, leaving the compound of formula (I).
CN102898433A Tetrandrine gallate and drug composition, preparation method and applications thereof The invention discloses tetrandrine gallate and a drug composition, a preparation method and applications thereof. The structure of tetrandrine is modified, and a novel derivative of the tetrandrine is prepared, namely, the tetrandrine gallate. Physical and chemical constant tests show that the solubility of the tetrandrine gallate is increased by 43 times than the tetrandrine. A pharmacology experiment shows that the tetrandrine gallate has an obvious inhibiting effect on the proliferation of tumor strain cells, and the effect is superior than that of the tetrandrine; and the tetrandrine gallate shows obvious blood pressure lowering, anti-inflammatory and pain easing effects which are higher than those of the tetrandrine, and the toxicity is smaller than that of the tetrandrine. Accordingly, the tetrandrine gallate is active ingredients and can be used for preparing anti-tumor, blood pressure lowering, anti-inflammatory and pain easing drugs, and the application range is wide.
US20090170925 Methods for prognosing the ability of a zearalenone analog compound to treat cancer The instant invention provides methods of prognosing the ability of a zearalenone analog compound to treat a cancer in a subject, methods of prognosing the ability of a zearalenone analog compound to inhibit the growth of a cancer in a subject, and methods of prognosing the ability of a zearalenone analog compound to promote the activation of apoptosis of a cancer in a subject. Methods of treating a cancer in a subject are also provided. The invention also pertains to methods of determining whether a cancer in a subject is sensitive to treatment with a zearalenone analog compound.
WO2006013963A1 External preparation for nail An external preparation for nail which contains a hydrophobic film-forming agent, a water-soluble polymer being soluble in alcohol and an antifungal agent and is excellent in quick-drying properties, penetration properties and persistence.
US20100280112 Composition Enriched in Diglyceride with Conjugated Linoleic Acid The present invention relates to an oil composition containing a large amount of a. diglyceride of conjugated linoleic acid (CLA), and more particularly to an oil composition with body weight control, anticancer, antioxidation and immune enhancement functions, which is based on a diglyceride of conjugated linoleic acid resulted from an enzymatic reaction between conjugated linoleic acid obtained from edible oil and glycerol. The inventive oil composition comprises 40-95% by weight of diglycerides, 5-60% by weight of triglycerides, 0.110% by weight of monoglycerides, and 0.02-10% by weight of residues, in which the ratio of conjugated linoleic acid (CLA) to fatty acids contained in the total glycerides is 5-98%. The use of the oil composition provides high-added-value foods, pharmaceutical compositions and foodstuff additives with effects of anticancer, immune enhancement, antioxidation, antichlorestol, growth promotion and the like.
US7015210 Methods of treating ophthalmic disorders with epoxy-steroidal aldosterone receptor antagonists A method for treating or preventing ophthalmic disorders comprising the administration of one or more aldosterone receptor antagonists that contain a 9,11-epoxy moiety, such as eplerenone is disclosed. The method results in a reduction of intraocular pressure which treats or prevents the ophthalmic disorders. Among the disorders are intraocular hypertension, glaucoma, low tension glaucoma, age-related macular degeneration (AMD), macular edema, and diabetic retinopathy. As glucocorticoids and mineralocorticoids also cause the retention of ions, such as sodium and potassium, where aldosterone receptors are located, aldosterone receptor antagonists that contain a 9,11-epoxy moiety, such as eplerenone, also can be administered to modulate the intraocular concentration of ions. Thus, aldosterone receptor antagonists can be administered to maintain an intraocular ionic environment that is beneficial to intraocular cell survival.
CN101948442A Preparation method of linezolid and preparation thereof The invention relates to a preparation method of linezolid and a preparation thereof, in particular to a preparation method of a linezolid raw material and a freeze-dried powder injection thereof. The preparation method mainly comprises the following steps: (1) synthesizing 2(S)-1-amino-3-chloro-2-propanol hydrochloride; (2) synthesizing (S)-N-[2-acetoxyl-3-chloropropyl] acetamide; (3) synthesizing 3-fluoro-4-morpholinyl nitrobenzene; (4) synthesizing N-carbobenzoxy-3-fluoro-4-morpholinyl aniline; (5) synthesizing the linezolid; and (6) preparing the linezolid preparation. The freeze-dried powder injection of the linezolid for injection, which is prepared by the invention, effectively improves the stability of medicines so that the medicines have longer shelf life, can be transported more conveniently and are more favorable for clinical applications. Moreover, the method of the invention for preparing the raw material linezolid and the freeze-dried powder injection thereof is simple and effective and is suitable for large-scale industrial production.
US20090069338 Method for predicting skin sensitizing activity of compounds Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.
CN101785766A Lidocaine and chlorhexidine aerosol In order to overcome the defects of current medicines for treating mosquito/bug bite, skin abrasion, soft tissue injury and minor burn, shorten treatment period, reduce adverse reaction, achieve convenient carrying, enhance curative effect and lower the use amount of medicine, the invention obtains a novel Lidocaine aerosol after optimized screening, which contains Lidocaine, chlorhexidine acetate, benzalkonium bromide, vinyl pyrrolidone-vinyl acetate copolymer, acetic ester, ethanol and propellant. The aerosol plays a good role of treating mosquito/bug bite and skin injury and simultaneously reduces the stimulation on skin.
CN103006536A Preparation method of nimodipine solid dispersible medicament by supercritical fluid technology The invention relates to the technical field of medicines, and discloses a preparation method of a nimodipine solid dispersible medicament by a supercritical fluid technology. Nimodipine serving as an active component is uniformly mixed with a hydrophilic carrier material in a mass ratio of 1:2 to 1:15, and putting in a high-pressure kettle; introducing supercritical CO2 fluid at a temperature of between 30 and 80 DEG C and pressure of between 10 and 40MPa for 2-24 hours; and reducing the pressure to collect the product in the kettle. Compared with a physical mixture of the solid dispersant, a fusion method and a solvent method, the nimodipine solid dispersant prepared by the method is remarkably increased in in-vitro dissolution rate, which means that the prepared solid dispersant has a remarkable effect of promoting absorption of nimodipine; and the preparation method has the characteristics of simple preparation process, mild preparation condition, no organic solvent, environmental friendliness and the like, and industrial production is easy to realize.
CN1953757B Composition for cleaning intestinal canal A composition for intestinal-canal cleaning which contains, added thereto, a corrective comprising a liquid perfume and containing substantially no sugar. The composition is packed into a packaging container which comprises an inner layer made of a flexible thermoplastic polyolefin resin and, superposed thereon, a layer of a rigid thermoplastic polyolefin resin so as to prevent the liquid perfumefrom disappearing and which has a capacity sufficient to enable water for dissolving the composition for intestinal-canal cleaning to be put therein at time of use.
US20070238727 5-Substituted 1-Phenyl-1,5-Dihydro-Pyrido[3,2-B]Indol-2-Ones and Analogs as Anti-Virals Compounds of formula (I) the N-oxides, salts, stereoisomeric forms, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, a carbonyl derivative, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)-methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is (i) aryl substituted with a radical —COOR4; (ii) C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, substituted with aryl which is substituted with a radical —COOR4; (iii) C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, substituted with —NR5a—C(═NR5b)—NR5cR5d, —O—NR5a—C(═NR5b)—NR5cR5d, -sulfonyl-R6, —NR7R8, —NR9R10, a radical (a-1), (a-2), (a-3), (a-4), (a-5); or (iv) a radical of formula: (a-6), (b-2), —CpH2p—CH(OR14)—CqH2q—R15; —CH2—CH2—(O—CH2—CH2)m—OR14; —CH2—CH2—(O—CH2—CH2)m—NR17aR17b; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, a carbonyl derivative, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.
US20110111012 Nanomaterial wound dressing assembly Wound dressing assemblies and methods of producing the wound dressing assemblies. The wound dressing assemblies various comprise individual layers of nanomaterials that have been formed according to an electrospinning process. Each of the layers can have different characteristics and qualities. The invention also provides guidance in selecting materials to form a wound dressing assembly, as well as possible adaptations to the electrospinning process to provide different characteristics for particular materials.
CN103503867A Production method for strong glutaraldehyde solution The invention discloses a production method for a strong glutaraldehyde solution which belongs to the field of antiseptic disinfectants. The strong glutaraldehyde solution is prepared from concentrated glutaraldehyde, a quaternary ammonium salt, a medicinal reinforcing agent and drinking water through blending, dissolving, split charging and the like. The method has the following main advantages: general equipment is used, the method is simple, product quality is good, poisonous and harmful gas and liquid are not discharged, and the produced strong glutaraldehyde solution can be mixed with water or ethanol at any ratio and is an excellent disinfectant and antiseptic drug; the strong glutaraldehyde solution is applicable to disinfection of medical instruments, animal stalls and body surfaces of animals, wherein the strong glutaraldehyde solution diluted 50 times is used to soak the medical instruments for 10 to 20 h so as to realize disinfection of the medical instruments, the strong glutaraldehyde solution diluted 500 times is sprayed for disinfection of the animal stalls, and the strong glutaraldehyde solution diluted 2000 times is used for disinfection of the body surfaces of livestock and poultry.
CN103610654A Micronized tinidazole powder injection The invention relates to a micronized tinidazole powder injection, which is prepared by the following steps: firstly, carrying out large-tray freeze-dried aseptic treatment on tinidazole and auxiliary materials, then micronizing by adopting a superfine grinding technology, so as to prepare fine powder, and carrying out aseptic packaging; or firstly, micronizing the tinidazole by adopting the superfine grinding technology, so as to prepare fine powder, carrying out large-tray freeze-dried aseptic treatment on the fine powder and the auxiliary materials, and carrying out aseptic packaging. By adopting the micronized tinidazole powder injection prepared by adopting the superfine grinding technology, the water solubility of the tinidazole is improved, the bioavailability is improved, and the clinical treatment effect of a medicament preparation is improved.
CN1854130B Chinazoline derivative, its production, medicinal composition and use A chinazoline derivative, its production, medicinal composition and use are disclosed. The composition comprises its medicinal salt, its hydrate and solvate, its polycrystal and copolycrystal. It can be used for anticarcinogenic and antiproliferative medicines.
US20110178074 Antipathogenic benzamide compounds The present invention is related to methods of treating bacterial infections in mammals using antipathogenic benzamide compounds having the formula wherein at least one of the R1 groups is F, Cl, CN or CF3 and R2, R3, Y, Z, m, and n are as defined herein.
CN101987170A Externally applied cream for repairing skin tissues and removing spots The invention relates to an externally applied cream for repairing skin tissues and removing spots, which is quite suitable for removing various color spots and can repair skin tissues and remove spots without any side effects. The external applied cream for repairing skin tissues and removing spots comprises the following components: 5%-10% of evonymun alatus, 5%-10% of rltalaindica, 5%-15% of licorice root, 5%-15% of unprepared rehmannia, 5%-15% of acnoitum kusnezoffii reichb, 2%-5% of astragalus mongholicus, 7%-10% of Chinese thorowax root, 7%-10% of white paeony root, 10%-15% of angelica, 4%-5% of nacre powder, 7%-10% of bletilla, 7%-10% of fleece-flower root, 10%-15% of dahurian angelica root, 10%-15% of poria, 7%-10% of rhizoma typhonii, 4%-5% of Japanese ampelopsis Root, 4%-5% of lithargite and 7%-10% of white atractylodes rhizome.
US20110287029 Inhibition of the beta3 subunit of l-type ca2+ channels The present invention provides reagents and methods for identifying inhibitors of the L-type Ca2+ channel β3 protein, which has been demonstrated to be involved in calcium signaling, insulin secretion, and glucose homeostasis. The invention also provides therapeutics and methods for treating a subject with one or more of diabetes, insulin resistance, impaired insulin secretion, and impaired glucose homeostasis, involving the use of inhibitors of an L-type Ca2+ channel β3 subunit to provide a benefit to the subject.
US20100190791 Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners The present invention relates to heterocyclic compounds that bind to Bcl proteins and inhibit Bcl function, compositions comprising such compounds, and methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
CN103340875A Application of compound in preparation of medicine for preventing or treating pancreatic fibrosis The invention discloses an application of Aspeverin in preparation of a medicine for preventing or treating pancreatic fibrosis, which is disclosed for the first time. The Aspeverin is of a completely new skeleton type and has the unimagined inhibiting activity to the pancreatic fibrosis, so that the possibility of hints from other compounds does not exist. Thus, Aspeverin has the prominent substantive characteristics; and the significant progress is achieved obviously when Aspeverin is used for resisting the pancreatic fibrosis.
EP1569665A2 Composition and method for mammary disinfection during winter conditions Improved aqueous, ready to use iodine teat dip compositions are provided which are specially formulated for winter time use to permit application to cows teats without freezing while at the same time affording adequate germicidal activity. The compositions include from about 0.01-2 % by weight iodine, from about 0.01-3 % by weight iodide ion, and from about 35-75 % by weight of an additive selected from the group consisting of glycerin and a mixture of at least about 10 % by weight glycerin based upon the total weight of the composition and one or more C2-C7 polyhydric alcohols different than glycerin and each containing at least 2 hydroxyl groups, said composition containing no more than about 45 % by weight propylene glycol when propylene glycol is one of said polyhydric alcohols. The compositions preferably have free iodine values of from about 1-60 ppm at 25° C and from about 0.5-20 ppm at 4° C.
EP2757157A1 Modulation of mitophagy and use thereof The present invention relates to an agent or composition comprising at least one of: (i) a micro-RNA targeting a mitophagy-associated gene or a variant thereof, (ii) a vector comprising a nucleic acid encoding said micro-RNA or variant thereof, (iii) an inducer of said micro-RNA, and (iv) an inhibitor of said micro-RNA, for use as a medicament. In particular, the invention relates to substances and compositions useful in the treatment of mitochondria-related diseases, in a subject, or to enhance protocols of in vitro production of red blood cells.
CN103450184A Salt of scoulerine derivatives The invention relates to fumarate of scoulerine (I) and scoulerine derivatives or solvate thereof, which can be accepted in pharmacology, and applications of the fumarate in preparation of drugs for curing hepatitis B virus infection.
US20100092441 Use of nitrites and nitrates and compositions containing these Inorganic anions nitrate and nitrite influence metabolic rate and glucose homeostasis. Infusion of nitrite iv caused an acute drop in resting energy expenditure (oxygen consumption) and nitrate, when given perorally, caused a drop in oxygen consumption during exercise and a depression of the increase in blood glucose observed after an oral glucose tolerance test. The doses of nitrate and nitrite did not cause any detectable change in methemoglobin levels of blood. Also, nitrate and nitrite did not alter lactate levels in blood. This discovery provides useful treatments to regulate the energy expenditure and glucose homeostasis of a mammal by administration of inorganic nitrite and/or nitrate.
CN101125179A Wound-healing muscle-growing ointment and production method thereof The present invention relates to a wound-healing and muscle-generating ointment and the production method thereof, the components of the pharmaceutical raw materials and the percentages by weight are: 17 to 20 percent baical skullcap root, 17 to 20 percent amur corktree bark, 17 to 20 percent liquoric root, 17 to 20 percent bletilla striata, 17 to 20 percent sinkiang arnebia root, 1 to 1.5 percent borneol and 6 to 6.5 percent borax. The production method is that the baical skullcap root, amur corktree bark, liquoric root and bletilla striata are cleaned and then dried for 4 hours at the temperature of 105 DEG C, after that, the four are smashed together with sinkiang arnebia root and then pass through a 120 mesh screen; the borneol and borax are added for even grinding, the ointment base is added, and the wound-healing and muscle-generating ointment is prepared by even grinding. The wound-healing and muscle-generating ointment preparation is used for changing the medicine for the traumas and infectious wounds, and the present invention has strong functions of antimicrobial, anti-inflammatory, generating muscle and promoting blood circulation, accurate efficacy and no adverse reactions. The production method is simple, the equipment requirements are low, so the prevent invention is applicable to the batch production of small and medium-sized pharmaceutical manufacturing enterprises and the preparation departments of the medical institutions.
WO2007036599A1 New crystallization process of quetiapine hemifumarate The present invention relates to a process for preparing crystalline quetiapine hemifumarate, which comprises crystallizing or re-crystallizing quetiapine hemifumarate from a mixture of water and a water soluble alcohol.
US7109202 Such as 3-(2-(6-methyl-pyridin-2-ylamino)-5-(1,2,4)triazol-1-yl-thiazol-4 -yl)benzonitrile for treatment of inflammatory or obstrucive airways diseases Compounds of formula (I) in free or salt form, where A is a C6-C15 monovalent aromatic group. R1 is hydrogen, phenyl optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, C1–C8-alkyl, C1–C8-haloalkyl, C1–C8-alkoxy, C1–C8-alkoxy-C1–C8-alkyl or acyloxy, or a 5- or 6-membered monovalent heterocyclic group, R2 is hydrogen, C1-C8-alkyl, acyl or CON(R3)R4, provided that R2 is C1–C8-alkyl, acyl or CON(R3)R4 when R1 is hydrogen, R3 and R4 are each independently hydrogen, or C1–C8-alkyl, together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, and Zl, Z2, Z3 and Z4 are each independently N or CR5, at least one of them being CR5, and R5 is hydrogen, C1–C8-alkyl or C1–C8-alkoxy. The compounds are useful as adenosine receptor antagonists, particularly in the treatment of inflammatory or obstrucive airways diseases
CN1827096A Docetaxel liposome containing chitosan derivative, lyophiled preparation and preparation method thereof The invention relates to a docetaxel liposome containing chitosan derivative, lyophiled preparation and preparation method, which comprises Docetaxel 1 part, chitosan derivative 1-10 parts, phospholipids 10-50 parts, and cholesterin 1-10 parts, The invention realizes stabilized quality, higher encapsulation efficiency and better effect.
CN101027054A Inhibitors of HSP90 The invention relates to the use of benzoimidazolone compounds and salts thereof in the treatment of proliferative diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, pharmaceutical preparations comprising benzoimidazolone compounds, novel benzoimidazolone compounds, and a process for the preparation of the novel benzoimidazolone compounds.
EP2455077A1 Prophylactic and/or therapeutic agent for dysmenorrhea Disclosed is a prophylactic and/or therapeutic agent for dysmenorrhea and/or associated symptoms thereof. Specifically disclosed is a prophylactic and/or therapeutic agent for dysmenorrhea and/or associated symptoms thereof, which comprises tranilast as an active ingredient thereof.
US8475828 Medical apparatus and method for producing same A medical device that includes at least one antibiotic in a macromolecular substance that swells upon contact with a solvent. Also, a method for preparing an antibiotic-containing medical device that involves contacting a medical device having at least a portion of the surface formed from a swellable macromolecular substance, with a solvent that swells the macromolecular substance, contacting the swollen macromolecular substance with at least one antibiotic, and removing the solvent from the swollen macromolecular substance.
EP1547585A1 Therapeutic agent for rheumatism containing benzamide derivative as active ingredient An object of the present invention is to provide a therapeutic agent for rheumatic diseases comprising a benzamide derivative as an active ingredient. The benzamide derivative according to the present invention is a compound represented by the following general formula [1] or a salt thereof as an active ingredient. In the formula, R1, R2 and R3, the same or different, are hydrogen, halogen, hydroxyl, lower alkyl, lower alkoxy, aryl, aryl-lower alkyl, aryloxy, amino, amino-lower alkyl, lower alkylamino or carboxyl, X is aryl or a heterocycle, Y is a direct bond or lower alkylene wherein the lower alkylene can contain oxygen atom(s) in the group, and Z is a direct bond or lower alkylene.
US20130052145 Adhesive slow-release formulations for the local administration of curcumin Through the combined use of solvents with polyacrylic acid, it is possible to produce curcumin formulations that are stable in liquid form, while having both mucoadhesive and slow-release properties and ensure a solubility of the active ingredient of up to 15% (w/v).
CN102091029A Sulfadimidine solution and preparation method thereof The invention relates to a sulfadimidine solution and a preparation method thereof. The solution comprises the following components in parts by weight: 5-10 parts of sulfadimidine, 20-40 parts of N,N-dimethylformamide, 15-25 parts of polyoxyethylene ether castor oil, and 100 parts of water. The preparation method of the solution comprises the following steps: preparing 30 ml of the N,N-dimethylformamide, adding the sulfadimidine, and stirring until the sulfadimidine is dissolved; and then adding the polyoxyethylene ether castor oil, and stirring until the polyoxyethylene ether castor oil is dissolved; adding the water till the total volume is 100 ml, and stirring to obtain the clean solution. In the invention, the sulfadimidine solution is prepared by using an advanced nanometer technology; in the solution, a cosolvent is utilized to ensure that the sulfadimidine slightly dissolved in water to be dissolved the oil phase, and a proper amount of emulsifier is added to form a uniform system; and the sulfadimidine solution prepared by using the method provided by the invention can be dissolved in water in any proportion.
WO2006019114A1 Skin-lightening agent containing polyphenol compound A skin-lightening agent sufficiently effective in lightening the skin. Also provided is a melanin generation inhibitor which contains as an active ingredient a polyphenol compound derived from acerola, an acerola polyphenol fraction, or another polyphenol compound, and which may optionally further contain ascorbic acid or an ascorbic acid derivative as an active ingredient. The skin-lightening agent contains the inhibitor. A cosmetic composition, food or beverage composition, or medicinal composition is further provided which contains the inhibitor.
US20080300298 Honokiol Derivates For the Treatment of Proliferative Disorders The present invention provides novel honokiol derivatives, as well as pharmaceutical compositions containing the honokiol derivatives. These compounds and pharmaceutical compositions can be used in the prevention and/or treatment of cancer. In particular, honokiol derivatives, pharmaceutical compositions comprising the derivatives, and methods for their use in the treatment of myeloma are provided.
WO2012162365A1 Substituted sulfonamides useful as antiapoptotic bcl inhibitors Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.
CN101890150A Novel and special Likexiao The invention relates to a novel and special Likexiao, which is prepared from the following components: 25g of monkshood, 25g of radix aconiti agrestis, 35g of Arisaemaerubescens, 35g of Pinellia ternata, 30g of seedofnuxvomicapoisonnut, 15g of frankincense, 15g of myrrh, 21g of monkshood, 35g of Angelica sinensis, 35g of radix notoginseng, 30g of radix angelicae pubescentis, 40g of lycopodium clavatum, 45g of golden flower, 55g of garden balsam stem, 50g of Ligusticum wallichii, 90g of semen brassicae, 60g of rhizoma zingiberis, 40g of radix clematidis, 10g of menthol crystal, 5g of borneol and ethanol the concentration of which is 75% through the steps of grinding the above components except the ethanol the concentration of which is 75% into fine powder for later use, soaking for 36h by clean water, preserving the temperature, purifying, three-time heating, extracting, filtering and decoloring, extracting by ethanol, synthesizing to obtain a golden yellow liquid finished product, and adding penetrant to obtain the novel and special Likexiao which is a Reyun universal pain permeation palm moxibustion liquid.
US20070172447 Agent for preventing and/or treating tissue disruption-accompanied diseases The present invention relates to an agent for preventing and/or treating diseases accompanied by tissue disruption, which comprises a polypeptide having granulocyte colony-stimulating factor activity as an active ingredient, and a medicament for mobilizing a multipotent stem cell from a tissue into peripheral blood, which comprises a polypeptide having granulocyte colony-stimulating factor activity as an active ingredient.
CN103110656A Water-soluble vitamin freeze-dried preparation for injection and preparation method thereof The invention discloses a water-soluble vitamin freeze-dried preparation for injection. 1000 bottles of freeze-dried preparations are prepared from the following raw materials: 2.8-3.4g of thiamine mononitrate, 36-44g of nicotinamide, 4.4-5.4g of pyridoxine hydrochloride, 14.8-18.1g of sodium pantothenate compound, 4.4-5.4g of riboflavin sodium phosphate, 102-124g of sodium ascorbate, 54-66mg of biotin, 0.36-0.44g of folic acid, 4.5-6.0mg of vitamin B12, 0.4-0.6g of methyl p-hydroxybenzoate, 280-320g of glycine, 0.4-0.6g of ethylene diamine tetraacetic acid disodium salt and 2000-3000ml of water for injection. The stability of existing sodium pantothenate is obviously improved by the obtained sodium pantothenate compound, thus ensuring that the sodium pantothenate containing water-soluble vitamin freeze-dried preparation for injection has ideal stability and curative effect and further ensuring medication safety of the patients.
CN102641243A 7-ethyl-10-hydroxycamptothecine liposome for injection and preparing method thereof The invention belongs to the technical field of medicine and relates to a recipe of 7-ethyl-10-hydroxycamptothecine liposome for injection and a preparing method. The recipe disclosed by the invention comprises the following components: 7-ethyl-10-hydroxycamptothecine, phospholipid, cholesterol, a stabilizing agent, an emulsifying agent, a carrier, a freeze-drying protecting agent and a pH regulating agent. The preparing method comprises the following steps of: dissolving the main medicines in an organic solvent, dissolving the carrier in a water phase, dripping a carrier solution into the organic solvent under the condition of magnetic stirring of water bath, decompressing, removing the organic solvent and water, lowering the particle size by externally adding acting force after redissolving by using a hydrated medium, adding the freeze-drying protecting agent for freeze drying so as to obtain liposome powder and redissolving before using so as to obtain a 7-ethyl-10-hydroxycamptothecine liposome solution for injection. The 7-ethyl-10-hydroxycamptothecine liposome for the injection, which is prepared by the preparing method, has high encapsulating rate and favorable stability; and moreover, the production is easy to amplify.
WO2012006083A2 Targeted receptor-mediated sirna Embodiments of this disclosure encompass compositions and methods for the delivery of siRNAs to the cytoplasm of a cell by endocytosis. The compositions comprise molecular conjugates between a receptor ligand, most suitably a small molecule ligand, and an siRNA that when administered to an animal or human subject in need thereof, can modulate or relieve symptoms of diseases such as, but not limited to, Sjogren's Syndrome as well as inhibiting or reducing such cellular processes as apoptosis of glandular acinar cells that trigger or sustain Sjogren's Syndrome. The siRNA moiety can reduce caspase-3 levels when delivered to a salivary or lacrimal cell. The method for delivery of a molecular conjugate to a cell, comprises the steps of contacting with a cell with a molecular conjugate comprising a ligand characterized as having affinity for a surface receptor of the cell, and an siRNA moiety linked to the ligand; and maintaining the cell, or population of said cells, under conditions whereby the ligand specifically binds to a surface receptor of the cell or cells, whereupon the molecular conjugate enters the cell or cells by endocytosis, thereby delivering the siRNA moiety to the cytoplasm of the cell or cells.
EP2253620A1 Substituted 3-cyanoquinolines as protein tyrosine kinases inhibitors This invention provides compounds of formula 1 wherein R1, G1, G2, R4, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof, which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
WO2005005632A3 SMALL INTERFERING RNA SPECIFIC TO SUB-UNITS $G(A), $G(A)' AND $G(B) OF THE KINASE PROTEIN CK2, AND THE APPLICATIONS OF THE SAME The invention relates to small interfering RNA specific to sub-units α, α' and ß of the kinase protein CK2, and to the applications of the same, especially for treating cancer and viral illnesses.
US7595317 Antiarthritic agents; rheumatoid and osteoarthritis; corneal, epidermal, or gastric ulceration; tumor metastasis or invasion; periodontal disease; and bone disease; 4-[(2-methyl-4-quinolinyl)methoxy]-N-(1,3,5-trioxo-2,4-diazaspiro[5.5]undec-7-yl)benzamide trifluoroacetate, for example The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-α converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.
WO2011076869A1 Isolated green plant material The invention relate to an isolated green plant material comprising at least 0.1 mg/g (dry weight) of zeaxanthin, a method of producing such as material as well as different products comprising said material and the use of such material and products.
CN101757090B Medicine composite for treating avian infectious bronchitis nephritis as well as preparation method and application thereof The invention relates to a medicine composite for treating avian infectious bronchitis nephritis, which comprises the following components in percentage by weight: 5-20 percent of honeysuckle extract, 10-30 percent of isatis root extract, 20-30 percent of astragalus extract, 2-5 percent of probenecid, 5-8 percent of taurine, 10-30 percent of paracetamol and the balance of auxiliary materials. Theinvention has low cost, is convenient to use, can be directly added into animal feeds and drinking water, overcomes multiple disadvantages of other treatment drugs, has no toxic and side effects or drug residue, and meets the requirements of safety veterinary drugs and original animal source food safety protection.
EP1499299A2 Microparticle pharmaceutical compositions for intratumoral delivery Provided are microparticles including paclitaxel, methods for making them, and pharmaceutical compositions containing them. Also provided are methods of treating tumors including the step of intratumorally injecting the paclitaxel-containing microspheres of the present invention.
CN102688219A Sulforaphane microencapsulation method The invention discloses a sulforaphane microencapsulation method which comprises the following steps of: I, extraction of sulforaphane: performing digestion of the raw material crucifer to extract the sulforaphane, wherein the extraction concretely comprises the following steps of: A, grinding seeds; B, adding petroleum ether for degreasing; C, adopting phosphate buffer solution with pH value of 7.0; D, performing enzymolysis; E, adding an extractant for extraction; F, adding sodium sulfate and sodium chloride respectively, and filtering; G, performing vacuum concentration to remove the organic solvent; H, fixing the volume to 5,000ml with methanol; I, filtering with a 0.22-micron microfiltration membrane; and J, measuring the content of sulforaphane by liquid chromatography; and II, microencapsulation of sulforaphane: adding monoglyceride and sodium alginate into the composite wall material, adding the deionized aqueous solution, adding the sulforaphane while stirring, spray-drying and collecting the product. In the method disclosed by the invention, the extremely unstable sulforaphane liquid is synthesized into powdery solid particles through a microencapsulation method so as to obtain perfect stability.
CN101735150A Thiourea derivatives containing pyrromonazole ring, preparation method and use thereof The invention provides novel thiourea derivatives containing a pyrromonazole ring, which have the following general formula. In the formula, R1 is CH3, Cl, Br or H, R2 is CH3, Cl, Br or H, R3 is F, Cl, Br or H, and R4 is F, Cl, Br, CH3, OCH3, OH, NO2 or H. The novel thiourea derivatives containing the pyrromonazole ring in the invention have an obvious inhibiting effect on the cancer cell strain (KB) of the epicuticle of human oral cavity and human leukemia cell strain (K562). Thus, the thiourea derivatives of the invention can be applied to the preparation of antineoplastic drugs. The invention discloses a preparation method of the thiourea derivatives.
US20100151018 Sustained-release levetiracetam composition and preparation process A subject of the present invention is a novel formulation of levetiracetam making it possible to obtain a solid pharmaceutical composition, particularly intended for oral administration, for the sustained release of levetiracetam. A subject of the invention is also a process for the preparation of such a pharmaceutical composition.
US20120058959 Topical antiviral formulations The disclosure provides novel topical antiviral pharmaceutical compositions comprising one or more antiviral compounds and 2-deoxy-D-glucose in the form of lip-balms, creams and ointments. A specific embodiment discloses a lip-balm composition comprising acyclovir and 2-deoxy-D-glucose.
US7812004 For modifying and modulating the bacterial flora and the fermentation pattern of inulin in the large intestine; anticancer agents; dietary fibre effects, improved mineral absorption (calcium and magnesium), for treating osteoporosis The invention relates to novel inulin products and compositions thereof, to their manufacture, to their use for modifying and modulating the bacterial flora and the fermentation pattern of inulin in the large intestine of humans, mammals or other vertebrates, to their use for providing improved inulin-associated nutritional effects/benefits, as well as to their use for the manufacture of consumer products and compositions for providing said effects/benefits in healthy, disfunctioned and diseased humans, mammals and other vertebrates. The novel inulin products consist of a particular mixture of an easily fermentable inulin (EFI) component and a hardly fermentable inulin (HFI) component. The nutritional effects/benefits include dietary fiber effects, improved mineral absorption, particularly calcium and magnesium, bone mineral density increase, reduction of bone mineral density loss, modulation of lipid metabolism, stimulation of the immune system, and anti-cancer effects. The novel inulin products are particularly suitable for the manufacture of a composition or a medicament for preventing, for postponing and/or for treating osteoporosis in humans, particularly in post-menopausal women and elderly people.
US20090074751 Growth factor fraction compositions and methods Compositions and formulations are provided comprising a growth factor fraction and at least one glucan. Also provided are methods for making the compositions and formulations. Methods of promoting growth in an animal using the compositions and/or formulations are also provided.
WO2013191763A1 Compositions containing theobromine and their use in treating tooth hypersensitivity Compositions and methods for reducing oral sensitivity, increasing the systemic health of a mammal, occluding a dentinal tubule within a mammalian tooth, and/ or depositing a precipitate on the surface of a mammalian tooth are provided, said compositions comprising theobromine (3,7-dimethylxanthine, the principal alkaloid in Theobroma cacao).
US7521042 Antihistamines, bronchodilator agents, antiinflammatory agents; mixture of drug and propellant The present invention relates to novel pharmaceutical aerosol formulations comprising: (A) a therapeutic agent in the form of particles coated by at least one coating excipient and at least one surfactant, in suspension in (B) a liquefied propellant gas for the administration of therapeutic agents particularly by the pulmonary route and to process for preparing these formulations. It also relates to novel particles suitable for use in such formulations.
CN103705462A Oral testosterone ester preparation and method for treating testosterone deficiency comprising oral testosterone ester preparation The invention provides an oral pharmaceutical composition which comprises testosterone undecanoate dissolved in a carrier, wherein the carrier comprises at least one oleophylic surfactant and at least one hydrophilic surfactant according to a ratio of total oleophylic surfactants to total hydrophilic surfactants in a range from about (6:1)-(3.5:1); the dissolved testosterone undecanoate comprises 18-22 weight percent of the composition. The invention also provides a pharmaceutic preparation of testosterone undecanoate. The invention further provides a method for treating testosterone deficiency or symptoms thereof by using the preparation. According to the treatment method comprising the oral pharmaceutical composition, because the preparation provides an optimal testosterone level, males suffering from hypogonadism can be clinically and effectively treated in a prolonged period of time.
CN102574844A Maleic acid salt and crystal thereof Disclosed is a benz[d][1,3]oxazine derivative having excellent stability when used as an active ingredient for a medicinal agent, and also having excellent solubility and crystallinity. Specifically disclosed is 2-[2-((S)-3-dimethylaminopyrrolidin-1-yl)pyridine-3-yl]-5-ethyl-7-methoxy-4H-benz[d][1,3]oxazin-4-one maleate.
CA2391834C Macrolide antibiotics and treatment of pasteurellosis 20,23-disubstituted mycaminosyltylonolide derivatives and use of the same in the field of the prophylaxis and treatment of pasteurellosis are disclosed. The di-sub-stituents are peperidino optionally substituted with one or two methyl groups. The derivatives have selective antibacterial activity against Pasteurella.
WO2012040923A1 Tetracyclic indole derivatives and methods of use thereof for the treatment of viral diseases The present invention relates to novel Tetracyclic Indole Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', G, R1, R15, U, V, V', X, X', Y and Y' are as defined herein. The present invention also relates to compositions comprisingat least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing HCV infection in a patient.
US20090029969 1-(2,4-dichlorophenyl)-4-methyl-5-(5-(pent-1-enyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide; cannabinoid receptor modulator; liver fibrosis, obesity, type II diabetes, atherosclerosis, analgesia, haemorrhagic shock, ischemia, liver cirrhosis, neurodegenerative diseases This invention relates to thiophene compounds of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to treat cannabinoid-receptor mediated disorders.
WO2014070771A1 Pyrimidine nucleotides and their monophosphate prodrugs for treatment of viral infections and cancer The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, cytomegalovirus (CMV), herpes viruses (HSV-1, HSV-2), Dengue virus, Yellow fever, or HBV in human patients or other animal hosts. The compounds are certain A^-hydroxycytidine nucleosides derivatives, modified monophosphate and phosphonates prodrugs analogs, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1, HIV-2, HCV, Norovirus, Saporovirus, cytomegalovirus (CMV), herpes viruses (HSV-1, HSV-2), Dengue virus, Yellow fever, and HBV.
US20100015061 Pharmaceutical Compositions Based on Anticholinergics and Andolast The present invention relates to novel pharmaceutical compositions based on anticholinergics and andolast, processes for preparing them and their use in the treatment of respiratory diseases.
WO2012024083A1 Oxathiazine and dithiine oxides as inhibitors of sulfhydryl-dependent biomolecules Novel derivatives of dihydro-l,4,2-oxathiazine and dihydro-l,4-dithiine oxides, more particularly, novel derivatives of dihydro-l,4,2-oxathiazine and dmydro-l,4-dithiine oxides that target cysteine residues of biomolecules of pharmacological importance are provided as pharmaceutically useful compounds, for example, as anticancer, antiinfectious, antigastric acid secretion, antiosteoporosic, and antiinflammatory agents.
WO2009149317A2 Transmucosal delivery of therapeutic agents and methods of use thereof Described herein is a transmucosal delivery device and their use for delivering bioactive agents across a mucosal membrane. The delivery devices contain a pharmaceutically acceptable oxidizing and agents that facilitates the delivery of the blood stream across the mucosal membrane.
US6964946 Oral pharmaceutical compositions containing taxanes and methods of treatment employing the same Pharmaceutical compositions for oral administration to mammalian subjects comprise a taxane or taxane derivative (e.g., paclitaxel or docetaxel) as active ingredient and a vehicle comprising at least 30% by weight of a carrier for the taxane, said carrier having an HLB value of at least about 10. The compositions may also comprise 0–70% of a viscosity-reducing co-solubilizer. The compositions may be incorporated into conventional oral pharmaceutical dosage forms, or can be in the form of a two-part medicament wherein the first part includes the taxane in a solubilizing vehicle and the second part comprises a carrier for the taxane to promote oral absorption. Methods of treatment of taxane-responsive disease conditions employing the novel compositions are also disclosed, whereby the compositions can be administered alone or in association with an oral bioavailability enhancing agent.
WO2011125911A1 Metal complexes and anticancer agents comprising same as active ingredient Provided are compounds which have reduced side effects (in particular, nephrotoxicity), compared with the existing anticancer agents such as cisplatin, and exhibit excellent anticancer activity. A metal complex represented by chemical formula (1): or a metal complex represented by chemical formula (2). In chemical formulae (1) and (2), each symbol has the meaning as defined in the description.
CN103272131A Preparation method of mouth cleaning care medicine in perioperative period The invention discloses a preparation method of a mouth cleaning care medicine in a perioperative period, which is used for preventing respiratory tract infection after an operation. The mouth cleaning care medicine is prepared from the following raw material medicines: fructus arctii, heterophyllous wingseedtree leaf, orange peel, cortex moutan, betel nut, rhizoma anemarrhenae, radix scrophulariae, rhizoma acori tatarinowii, honeysuckle, pinellia ternata, bamboo shavings, gypsum, rhizoma alismatis, radix glycyrrhizae preparata and clam meal. The preparation method comprises the following steps of: (1) extracting volatile oil for use from the fructus arctii, heterophyllous wingseedtree leaf, orange peel, cortex moutan, betel nut, rhizoma anemarrhenae, radix scrophulariae, rhizoma acori tatarinowii and honeysuckle; (2) decocting the pinellia ternata, bamboo shavings, gypsum, rhizoma alismatis, radix glycyrrhizae preparata and clam meal in water twice, and combining the decoctions; (3) filtering the decoction and performing ultrafiltration to obtain ultrafiltrate; and (4) spraying the mixed volatile oil into the ultrafiltrate, uniformly mixing, sterilizing and sub-packaging. Clinical experiments prove that the mouth cleaning care medicine in a perioperative period, prepared from the formula by the preparation method disclosed by the invention, can reduce respiratory tract infection when applied to mouth care before and after an operation, has good taste and deserves clinical application and popularization.
WO2010011626A3 Pyridinyl modulators of ϒ-secretase The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer's disease.
US20100324127 Treating neurodegenerative diseases with progranulin The invention relates to methods and compositions for treating a neurodegenerative disease. More particularly, the present invention is directed to methods of treatment of neurodegenerative diseases using progranulin and progranulin polypeptides, and methods of treatment of neurodegenerative diseases using effectors, or combinations of effectors, that modify progranulin expression.
WO2007085420A1 Medicament comprising a hormone combination The invention relates to the use of a hormone combination of ethinyl estradiol or estradiol as an estrogen component and at least one chlormadinone acetate metabolite selected from the group comprising 3α-hydroxy-6-chloro-17α-acetoxy-4,6-pregnadiene-20-one (3α-hydroxy-chlormadinone acetate), 3β-hydroxy-6-chloro-17α-acetoxy-4,6-pregnadiene-20-one (3β-hydroxy-chlormadinone acetate), 3α-hydroxy-6-chloro-17α-acetoxy-5β-pregnane-20-one, and 3β-hydroxy-17α-acetoxy-5β-pregnane-20-one, optionally mixed with chlormadinone acetate as a gestagen component for producing a medicament that is utilized for at least alleviating mood swings related to the menstruation cycle and optionally as a hormonal contraceptive in women.
CN103272047A Infantile cold granules and preparation method thereof The invention discloses infantile cold granules which consist of the following raw materials: 65-70 parts of pogostemon cablin, 70-80 parts of fructus forsythiae, 75-78 parts of radix cynanchi atrati, 60-65 parts of rhizoma rehmanniae, 90-95 parts of gypsum, 8-10 parts of folium isatidis, 10-15 parts of folium mori, 30-40 parts of cortex phellodendri and 0-60 parts of radix puerariae. The invention also discloses a preparation method of the infantile cold granules. The infantile cold granules and the preparation method thereof disclosed by the invention have the advantages that a small dosage of the cold medicine is applied, the effect is obvious, and a little side effect is caused; the preparation technology has mild conditions and is fine; and with good stability and small dosage, the infantile cold granules are suitable for infants.
US20100305133 Prolyl Hydroxylase Inhibitors The invention described herein relates to certain quinoxaline-5-carboxamide derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
US20080214674 Acylhydrazone derivatives and the use thereof in the inhibition, regulation and/or modulation of kinase signal transduction Acylhydrazone derivatives of the formula (I) are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in any type of fibrosis and inflammatory process. In which R1, R5 each, independently of one another, H, OH, OA, OAc or methyl, R2, R3, R4, R6, R7, R8, R9, R10 each, independently of one another, H, OH, OA, OAc, OCF3, Hal, NO2, CF3, A, CN, OSO2CH3, SO2CH3, NH2 or COOH, R11H or CH3, A alkyl having 1, 2, 3 or 4 C atoms, X CH2, CH2CH2, OCH2 or —CH(OH)—, Hal F, Cl, Br or I.
WO2014093031A1 Bacteria targeting nanoparticles and related methods of use The present invention relates to bacteria-targeting nanoparticles and related methods of use. In particular, the present invention relates to dendrimer nanoparticles conjugated with Vancomycin and/or Polymixin (e.g., Polymixin B, Polymixin E). In certain embodiments, such dendrimer nanoparticles are used to sequester and/or identify bacteria (e.g., Gram-positive bacteria and/or Gram-negative bacteria), screen liquid samples (e.g., water samples, food samples, pharmaceutical samples, blood samples, blood platelet samples, etc.) for the presence of bacteria (e.g., Gram-positive bacteria and/or Gram-negative bacteria), treat disorders associated with bacteria (e.g., Gram-positive bacteria and/or Gram-negative bacteria), and/or identify, sequester, and remove bacteria (e.g., Gram-positive bacteria and/or Gram-negative bacteria) from a liquid sample (e.g., water sample, food sample, pharmaceutical sample, blood sample, blood platelet sample, etc.). In certain embodiments, iron oxide nanoparticles are coated with dendrimer nanoparticles conjugated with Vancomycin and/or Polymixin.
WO2007114922A3 Salts of 8-[{1-(3,5-bis-(trifluoromethyl) phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and preparation process therefor Disclosed are crystalline salt forms of (5S,8S)-8-[{(1 R)-1-(3,5-Bis- (trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-d;diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
CN102161619A Ferulic acid Jiangtang compound salt as well as preparation method and application thereof The invention relates to a ferulic acid biguanide compound salt as shown in a formula I. In the formula I, R is a biguanide Jiangtang compound. The invention also provides a preparation method, application and the like of the compound salt. The ferulic acid biguanide compound salt has the functions of reducing side effect and taking a synergistic effect, can be used for preventing and treating dabetes mellitus and has the functions of preventing and treating Diabetic complication-diabetic nephropathies.
CN103417699A Drug for treatment of impetigo and preparation method thereof The invention relates to drug for the treatment of impetigo and a preparation method thereof. The drug is made by grinding rhubarb, gypsum rubrum, talc, natural indigo, gypsum, corktree bark, dried alum and coptis root, screening with a 200-mesh screen, adding a proper amount of sesame oil to prepare paste, and packaging to obtain finished products. The drug is low in cost, free of oral administration and convenient to use, has no toxic and side effects, and is significantly effective in treating impetigo.
WO2012067269A1 Aminoalkoxyphenyl compounds and their use in the treatment of disease The invention concerns compounds of Formula (I): (I) wherein n, m, p, R1 and R2 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, novel intermediates useful in the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of disease, for example cancer.
WO2014116962A1 Selective histone deacetylase 8 inhibitors Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that benefit from inhibition of HDAC8 activity
WO2013149091A1 Composition and method for treating neurodegenerative disease The present invention provides a method and composition for treating a neurodegenerative disease. In particular, the present invention provides a method and composition to increase DJ-1 gene expression or DJ-1 protein activity to treat a neurodegenerative disease.
US20080070961 storage stability; precipitation N-(2-acetyl-4,6-dimethylphenyl)-3-([(3,4 dimethyl-5-isoxazolyl)aminosulfonyl}-2-thiophenecarboxamide, is provided here in the form of three polymorphs (Forms A, C and E). Forms A, C and E are specified by their peaks in their X-ray powder diffraction patterns, their absorption peaks in their infrared absorption spectra in potassium bromide, their peaks in their Raman absorption spectra, or their melting points.
US6989270 Using polyamide nucleic acid oligomers to engender a biological response The invention involves methods and materials for extracellularly administering PNA oligomers to living cells. Specifically, the invention provides methods and materials of treating living cells with PNA oligomers such that the oligomers cross biological barriers and engender a biological response in a sequence specific manner. In addition, the invention provides methods and materials for orally administering PNA oligomers to animals such that the oligomers cross biological barriers and engender a biological response in a sequence specific manner. The invention also provides sense and antisense PNA oligomers that modulate transcription and translation, respectively. The invention also provides mismatch PNA oligomers that modulate the degree of an engendered biological response. In addition, the invention provides methods and materials for detecting PNA oligomers within a biological sample collected from an animal. Further, the invention provides methods and materials for screening potential PNA oligomers for the ability to engender a sequence specific biological response. Further, the invention provides methods of identifying the function of polypeptides and of determining the relative turnover rate of functional polypeptides.
EP1221852B1 Therapeutic use of antimicrobial compositions comprising a benzoic acid analog and a metal salt The present invention relates to antimicrobial compositions which provide enhanced immediate as well as residual anti-viral and antibacterial efficacy. The antimicrobial compositions of the present invention provide previously unseen residual effectiveness against Gram negative bacteria, Gram positive bacteria, and viruses, fungi, and improved immediate germ reduction upon use. These compositions comprise: (a) a safe and effective amount of a benzoic acid analog; (b) a safe and effective amount of a metal salt; and (c) a dermatologically acceptable carrier for the acid and salt wherein said composition has a pH of from about 1 to about 7. The invention further relates to methods of use for the present compositions as well as antimicrobial products which incorporate the compositions.
WO2005094812A1 Nateglinide-containing preparation It is intended to provide a nateglinide-containing preparation (in particular a preparation disintegrated in the oral cavity) having a lessened bitterness which is a medicinal composition containing nateglinide as the active ingredient and characterized by further containing at least one member selected from the group consisting of organic acids, inorganic acids, sweeteners and perfumes.
CN101228935A Weight-losing and antidiabetic instant rice The invention relates to a food used for reducing weight and glucose. The invention aims at inventing a kind of food which is convenient for eating and also has the effects of reducing weight and glucose, and through eating which can reach the aims of losing weight and reducing glucose of human body. The invention is realized by that the invention is made by compound rice, and the compound comprises 0.45 percent to 1.8 percent of stearic acid single acylglycerol, and 0.05 percent to 0.2 percent of sucrose fatty acid. Calculated by a weight percentage, the compound accounts for 0.5 percent to 2 percent and the rice accounts for 99.5 percent to 98 percent. The detail embodiment for implementing the invention relates to putting the compound into the rice after dipping the rice for 1 hour, flushing the rice with hot water of 60 DEG C and then flushing with cold water of 10 DEG C after the rice is cooked, and then freezing and drying the rice in a freezer, or baking and drying the rice in a bake oven.
US20080293656 Processing nucleic acid The present invention relates to a method of processing nucleic acid. More particularly, it relates to a method of purifying extra-chromosomal DNA by removing cell debris and/or RNA from a process stream comprising extra chromosomal DNA and a precipitate resulting from preceding cell lysis and/or precipitation reactions. It also relates to nucleic acid, particularly extra chromosomal DNA, purified by a method of the invention; a pharmaceutical composition comprising or consisting of the same and apparatus for said method. The method comprises: Controlling the cell lysis and/or precipitation reactions to substantially minimise the formation of small particles and/or maximise the formation of large particles; and Straining the process stream by passing it through a mesh or sieve with a mesh size of greater than 75 μm to remove a substantial % mass of the precipitate from the process stream.
US20120295977 Organosulfur prodrugs for the prevention and treatment of infectious diseases A method for enhancing the overall beneficial immune system response in a host that works in conjunction with the host's natural immune system response to enhance the host's ability to eliminate infectious microbes while simultaneously suppressing the toxicity of the immune system response to the host. Allium related organosulfur compounds are disclosed which have a various antimicrobial immunomodulatory properties that work together with the host's immune system in the prevention and treatment of disease. Prophylactic and therapeutic treatment is provided by administering an allium related organosulfur compound such that a localized thiosulfinate is caused to be non-enzymatically formed in response to localized generation by activated immune system cells of reactive oxygen species such as hydrogen peroxide. Suitable allium related organosulfur compounds may be administered to the host in an efficient manner through the use of S-AllylMercapto-N-AcetylCysteine (SAMNAC) or similar prodrugs.
EP1902756A1 Composition and method for treating skin by administering silybin and piperine/terahydropiperine Suggested are cosmetic compositions comprising in a cosmetically acceptable excipient (a) silybin and (b) piperine and/or tetrahydropiperine. The compositions are suitable for preventing and/or soothing dry skin or reactive skin against external stresses.
WO2014140680A1 Dosing regimen for use of celgosivir as an antiviral therapeutic for dengue virus infection Methods of treating a dengue virus (DENV) infection in a human subject, comprising administering to the human subject a compound of Formula (I), or pharmaceutical composition comprising a compound of Formula (I): A compound of Formula (I) can be administered within 48 to 72 hours of fever onset due to dengue infection and then every.6 to 1-2-hours until there is an improvement in the infection. The methods of the invention can be used to treat primary and secondary DENV 1-4 viral infections.
CN101296695A Combinations comprising AMXAA for the treatment of cancer The present invention relates to combinations of the xanthenone acetic acids class such as 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and EGFR signalling pathway inhibitors. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations.
US20100234390 Novel compound and their use The present invention provides novel compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof. The novel compounds are useful as antibacterial agents in the treatment of conditions such as nosocomial pneumonia, community acquired pneumonia, infections caused by vancomycin resistant enterococci (VRE), methicillin resistant Staphylococcus aureus (MRSA), Heamophilus influenzae (HI) and penicillin resistant Streptococcus pneumoniae (PRSP). The compounds of the present invention are effective against a number of human or animal pathogens including VRE, PRSP, HI and MRSA.
WO2010056527A3 B-biphenyl sulfonamide compounds as ion channel modulators The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
EP2089350A1 Crystalline potassium salt of lipoxin a4 analogs This invention is directed to the crystalline potassium salt of a lipoxin A4 analog of Formula (I): processes for preparing the crystalline potassium salts, methods for using them to treat disease-states characterized by inflammation, and pharmaceutical compositions comprising such crystalline potassium salts.
WO2008124550A1 Phenothiazin derivatives for antiviral treatments Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C.
US20090110656 Skin cooling composition A cooling composition for application to the skin of a mammal, such as a human. The base of the composition is an interpenetrating polymer network, which may contain a thermo-responsive polymer. Having a Critical Temperature above an average core body temperature, the material may undergo a phase change as the creature becomes too warm, such as when a person experiences a hot flash, a fever, exposure to very warm environments, physical exertion, and the like. The phase change results in a cooling and/or cooling sensation of the skin. Additives may be included in the cooling composition such as evaporative cooling components, neurosensory cooling components, and additional phase change components.
CN101108170A Aceclofenac in extended-released tablets and method of manufacturing the same The invention relates to a drug sustained-release preparation and its preparation method, in particular to an aceclofenac sustained-release tablet and its preparation method, which comprises the following ingredients according to the weight percentage: aceclofenac of 60 to 95 per cent, skelecton retarder of 3 to 30 per cent, adhesive of 1 to 10 per cent and lubricant of 0.5 to 15 per cent. The hydroxypropylmethyl cellulose and carboxyvinyl polymer are adopted as optimized skelecton retarder. With such a technical proposal in the invention, the one aceclofenac sustained-release tablet can be taken a day to effectively reduce the fluctuation of blood drug level, prolong the maintenance duration of effective blood drug level and lower down the incitement to gastrointestinal tract. Besides, the invention also provides the preparation method of the aceclofenac sustained-release tablet.
CN103223152A Medicine for treating infertility caused by uterus coldness The invention discloses a medicine for treating the infertility caused by uterus coldness. The medicine is characterized in that the medicine comprises 4-8 parts of Chinese angelica, 5-15 parts of Cassia Twig, 4-14 parts of Herba Leonuri, 6-12 parts of donkey-hide gelatin, 6-12 parts of Ligusticum wallichii, 6-12 parts of safflower, 6-12 parts of Radix Polygalae, 6-12 parts of Sappanwood, 4-8 parts of Artemisia argyi, 2-6 parts of Fructus Amomi, 8-12 parts of Fructus Evodiae and the like, wherein Cassia Twig, safflower, Fructus Evodiae, Rhizoma Cyperi and fluoritum are used as primary medicines, the residual above components are auxiliary medicines, and all the above components complement each other to realize advantage drawing and shortage offsetting, efficacy enhancing and toxic and side effect attenuating effects. The medicine has the efficacies of cold dispelling, stasis removing, blood circulation invigorating, blood enriching, pregnancy assisting, miscarriage preventing and the like, and can effectively treat the infertility caused by uterus coldness, and symptoms comprising abnormal menstruation, amenorrhea, dysmenorrheal and asthenia cold abdominalgia and caused by the uterus coldness.
CN1947703A Stable elaioplast compositions A stable liposome composition used as the carrier of anticancer medicine taxol is prepared from saturated phosphatide, cholesterol, VE and cane sugar through thin-film evaporation and freeze-drying.
WO2013121452A8 Product comprising glucomannan and chitosan for the treatment of gastroesophageal reflux disease A nutraceutical preparation and/or food supplement and/or medical device product for the use in the treatment of gastric reflux comprising the association of glucomannan and an organic base, chitosan, and optionally one or more carbonates.
US8835482 Substituted indazole and aza-indazole derivatives as gamma secretase modulators The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I) wherein R1, R2, R3, R4, Y, A1, A2, A3, A4, X1, X2, X3 and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
US20110207789 Methods related to casein kinase ii (ck2) inhibitors and the use of purinosome-disrupting ck2 inhibitors for anti-cancer therapy agents Disclosed are methods related to label-free biosensor cellular assays to classify multienzyme complex modulators in live cells. Disclosed are also methods related to the identification of purinosome disrupting Casein Kinase II (CK2) inhibitors, and methods related to the use of purinosome disrupting CK2 inhibitors as therapeutic agents for modulating CK2 activity and purine synthesis pathway, and for improving prevention and treatment of CK2 associated cancers, viral infection and inflammation conditions.
EP2412372A1 2-Aminooxazole derivatives for use as TRPV1 antagonists for treating i.a. pain, inflammation, neurodegenerative diseases or gastrointestinal diseases Compounds of formula (I) wherein R1, R2, R4, and W are defined in the description are TRPV1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
CN101797377A Fibrin sealant and preparation method thereof The invention provides a fibrin sealant which comprises a fibrin polymer and a thrombin-like enzyme, wherein a ratio of the thrombin-like enzyme to the fibrin polymer is 0.01 to 100 IU:1 mg. The fibrin sealant can be used on the aspects of hemostasis, healing promotion, defect enclosing, bonding prevention, tendon suture fixation tendon injury, molding repair of bony defect, regeneration of skin tissue, carrier slow release and the like.
WO2014065572A1 Pharmaceutical composition for preventing or treating cancer, containing enoblock as active ingredient The present invention relates to ENOblock, which is a non-substrate analogue having an enolase inhibitory activity, and a pharmaceutical composition for preventing or treating cancer or enolase-associated diseases, containing the same. The ENOblock of the present invention directly binds to enolase so as to inhibit an activity thereof, and the inhibition is more effective in hypoxia than in normoxia. In addition, the ENOblock of the present invention inhibits migration, metastasis and invasion of cancer cells. Furthermore, the ENOblock of the present invention induces glucose uptake into cells, down-regulates the expression of PEPCK, and inhibits adipogenesis and foam cell formation. Therefore, a composition containing the ENOblock of the present invention can be very effectively applied to prevent or treat cancer or enolase-associated diseases.
CN103212055A Drug composition of bortezomib and preparation method thereof The invention belongs to the technical field of medicines and particularly relates to a drug composition of bortezomib and a preparation method thereof. The drug composition disclosed by the invention contains bortezomib, tert butyl alcohol, sodium chloride and an excipient in the mass ratio of 1:0.5:(1-5):(5-20). The drug composition adopts freeze-dried powder injection or water injection, preferably the freeze-dried powder injection. The drug composition contains tert butyl alcohol and sodium chloride besides the conventional excipient; through adding tert butyl alcohol, bortezomib can be rapidly dissolved and rapidly reacted with polyalcohol excipients such as mannitol to form more stable borate, so that the stability problem of the bortezomib freeze-dried powder injection per se is solved; and through adding the drug active constituent i.e. sodium chloride, the normal physiological and biochemical activities and functions in vivo are fully guaranteed.
CN101732320A Novel medicinal composition for relieving cough The invention discloses a medicinal composition capable of relieving cough and reducing sputum and a production method thereof. The composition is especially used for treating cough symptoms in the diseases of the respiratory system, such as influenza, whooping cough, bronchitis, laryngitis and the like. A medicine prepared from the composition comprises the following effective components in unit dose: 0.01-20mg of pholcodine, 0.1-300mg of guaiphenesin and 0.01-20mg of maleic acid/or hydrochloride chlorpheniramine. The medicinal composition is an oral preparation. Compared with the similar medicine, the medicinal composition has the characteristics of small dosage, favorable curative effect, high safety and convenient taking.
CN101597217A PTP1B inhibitor as well as synthesis method and application thereof in preparation of medicine for curing type 2 diabetes The invention relates to a novel chemical synthesis method of PTP1B inhibitor and the application thereof in the medicine for curing type 2 diabetes, wherein the PTP1B inhibitor has a chemical structural formula as follows: wherein a group connected with 2 site, 2' site and 3 site carbon of benzene ring is bromine atom; 4,4' and the number 5, 5' carbon of the benzene ring are connected with methoxyl; and the PTP1B inhibitor has a chemical name in English: (2'-bromo-4',5'-dimethoxy-phenyl)-(2,3-dibromo-4,5-dimethoxy-phenyl)-methane. The compound can enhance the sensibility of insulin receptor by restricting the activity of protein tyrosine phospholipase 1B and has favorable curing effect for type 2 diabetes in insulin resistance types.
US20080045467 Composition Containing Ginsenoside F1 Or Compound K For Skin External Application The present invention relates to an inhibitor for the biosynthesis of gelatinase comprising ginsenoside F1 (20-O-β-D-glucopyranosyl-20(S)-protopanaxatriol) or compound K (20-0-β-D-glucopyranosyl-20(S)-protopanaxadiol), which is a chief metabolite of ginseng saponin, as an active ingredient; and a cosmetic/medical composition for the prevention of skin-aging comprising the same which is superior in inhibiting the decomposition of epidermal-dermal junction and also in accelerating the generation thereof.
CN1615830A Amfepramone hydro chloride dripping pill The present invention discloses slimming medicine composition, and is especially orally taken medicine composition dripping pill with Amfepramone hydrochloride as active component. The present invention aims at providing Amfepramone hydrochloride dripping pill with great medicine carrying amount, fast medicine release, quick acting, high bioavailability, less toxic side effect, convenient use and low cost. Amfepramone hydrochloride as active medicine component is mixed with medicine carrier as matrix, and the mixture is heated until obtaining medicine composition molten liquid and/or emulsion and/or suspension, which is dropped into condensating agent in dripping pill machine to contracting form.
WO2011058113A1 Fused bicyclic pyridine and pyrazine derivatives as kinase inhibitors A series of fused bicyclic pyridine and pyrazine derivatives, substituted directly on the pyridine or pyrazine ring by a functional group attached via a sulphur-containing linkage, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
CN102438613A Anti-inflammatory composition containing macrolactin a and a derivative thereof as active ingredients The present invention relates to an anti-inflammatory use of macrolactin compounds such as macrolactin A, 7-O-malonyl macrolactin A, and 7-O-succinyl macrolactin A, which are produced from a novel Bacillus strain of Bacillus polyfermenticus KJS-2 (KCCM10769P). The macrolactin compounds provided by the present invention were confirmed to greatly suppress the expression and growth of inducible nitric oxide synthetase (iNOS) and cyclooxygenase-2 (COX-2) which are proteins related to the formation of inflammatory mediators, and to accordingly inhibit the formation of nitric oxide (NO) and of prostaglandin E2 (PGE2) which are the metabolites of the proteins.; In addition, the macrolactin compounds provided by the present invention were confirmed to have excellent effects in inhibiting the formation of tumor necrosis factor-alpha (TNF-a), which is a pro-inflammatory cytokine, interleukin-1ss (IL-1ss), interleukin-6 (IL-6) and granulocyte macrophage colony-stimulating factor (GM-CSF). Therefore, the macrolactin compounds produced by the Bacillus polyfermenticus KJS-2 strain according to the present invention can provide excellent anti-inflammatory agents.
CN103330858A Tibetan medicine used for treating cerebral thrombus and preparation method thereof The invention discloses a Tibetan medicine used for treating cerebral thrombus and a preparation method thereof. The Tibetan medicine is composed of an active ingredient, or the active ingredient and pharmaceutically acceptable accessories, wherein the active ingredient is prepared by mixing rosa multiflora, primula sikkimensis, corydalis pygmaea, corydalis pallid, pubicatulum, fructus choerospondiatis, gastrodia elata, borax, concretio silicea bambusae and safflower carthamus according to a ratio by weight. The medicine can be processed to be any kind of commonly used preparation for oral administration. The Tibetan medicine is capable of activating blood circulation and removing stasis, and resisting thrombosis and dredging veins. The Tibetan medicine is used for treating cerebral thrombus, myocardial infarction, thrombophlebitis and thromboangiitis obliterans.
CN201223619Y Multifunctional integrated anaesthesia equipment for skin A multifunctional comprehensive skin anaesthetic apparatus is characterized in that a pre-anaesthetic device before skin operation and a continuous anaesthetic device used during the skin operation, wherein the pre-anaesthetic device consists of a tremble anaesthetic device, a freezing device and a herbal anaesthetic pad; the freezing device consists of a connection nut of a freezing anaesthetic device, a connection bolt of the freezing anaesthetic device, a spiral upper cover of the freezing anaesthetic device, a metal body of the freezing anaesthetic device and a spiral lower cover of the tremble anaesthetic device; the tremble anaesthetic device is connected with the connection bolt of the freezing anaesthetic device on the spiral upper cover of the freezing anaesthetic device through the connection nut of the freezing anaesthetic device; the herbal anaesthetic pad is arranged on the spiral lower cover of the freezing anaesthetic device; the continuous anaesthetic device consists of a tremble anaesthetic device and an electrode anaesthetic device; and the electrode anaesthetic device consists of an electronic pulse microprocessor, and a semi-circular low-frequency pulse metal electrode switch and a semi-circular low-frequency metal electrode electrically connected with the electronic pulse microprocessor. The multifunctional comprehensive skin anaesthetic apparatus can be widely used for anaesthesia for various small-area debridement and minor operations for bee therapy, skin test, needle insertion for infusion, small-area burn, scald, and furuncle without toxicity.
US20110020433 Compositions for delivery of cargo such as drugs proteins and/or genetic materials Compositions and methods for delivery of cargo molecules to a patient or subject in need thereof include a proteoliposome carrier vehicle that incorporates an RLIP76 protein and contains the cargo molecule. The vehicle effectively delivers the cargo molecule systemically throughout the tissues of the body including into the central nervous system.
US20090104119 Dendrimer Based Compositions And Methods Of Using The Same The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based multifunctional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
US20090275606 Heterocyclic Compounds as MEK Inhibitors The present invention relates to compounds of formula I and pharmaceutically acceptable salts. These compounds can act as potential MEK inhibitors in the treatment of hyperproliferative diseases, like cancer and inflammation. The present invention also reveals methods of preparation thereof.
CA2805567A1 Pyrimidine compounds as inhibitors of protein kinases ikk epsilon and/or tbk-1, processes for their preparation, and pharmaceutical compositions containing them C Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases ???e and/or TBK-1 : in which: R1 represents an aliphatic heterocyclyl group having 4, 5, 6 or 7 ring atoms, bonded to the phenyl group shown in formula I through a ring nitrogen atom, and optionally substituted by one or more substituents defined in the Specification; R2 represents a phenyl or heteroaryl group which is optionally substituted by one or more substituents defined in the Specification; and each of R3 and R4 independently represents a hydrogen atom or a C1-4 alkyl group.
CN1895243A Danshen-root ketone IIA oral-cavity disintegrating tablets An oral disintegrating tablet of danshinone IIA for the patients of cardiovascular and cerebrovascular diseases contains danshinone IIA, povidone, xylitol and/or sorbitol.
CN1561986A Capsule agent containing L-glutamine and azulene sodium solfonate A capsule containing L-glutamine (C5H10N2O3) and sodium azulenylsulfonate (C15H17NaO3S.1/2H2O) is disclosed.
WO2013144737A3 Novel 3,5-disubstitued-3h-imidazo[4,5-b]pyridine and 3,5- disubstitued -3h-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of c-met protein kinases The present invention provides compounds useful as C-met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of C-met kinase mediated diseases or disorders with them.
CN103735567A Composite hemostatic spray The invention discloses a composite hemostatic spray of the medical preparation field, the composite hemostatic spray comprises the following components: by weight, 0.3-1 part of alginic acid, 1-3 parts of hydroxypropyl chitosan, 0.5-5 parts of N, N-dicarboxymethyl chitosan, 0.5-5 parts of an anti-inflammatory analgesic and 10-30 parts of distilled water. The composite hemostatic spray has the advantages of being hemostatic, anti-inflammatory, wound healing promoting, anti-sticking, low-price, easy to use, and the like, and can be used for rapid hemostasis of various wounds, surgical wound surfaces, and other surface trauma.
CN1579415A Yuzu Sea-cucumber osamine glycan injecta and its preparation method The invention provides an injection solution for curing blood embolism diseases, it contains sea cucumber glycosaminoglycan. Above 93% of the sea cucumber glycosaminoglycan is the one with molecular weight of 100000-140000. The injection solution can be freeze-dry injection solution and water injection solution. The invention also provides the manufacturing method for above mentioned injection solution, it contains steps of crash, immerse, enzyme decomposing and depositing of sea cucumber.
CN103304604A Clindamycin phosphate compound and preparation method and pharmaceutical composition thereof The invention relates to a pharmaceutical compound, and particularly relates to a pharmaceutical compound of clindamycin phosphate and a preparation method and a pharmaceutical composition thereof. The X-ray powder diffraction pattern of the clindamycin phosphate compound, measured by use of Cu-K alpha rays, is shown by the figure 1. The clindamycin phosphate compound provided by the invention has good stability, does not absorb moisture easily and is very suitable for being prepared into various powder-needle dosage forms so as to fundamentally solve the problem of stability drop after moisture absorption; and a stability test proves that the lyophilized powder needle, large-volume injection and small-volume injection prepared from the clindamycin phosphate compound have good stability and are very suitable for clinical application.
EP1343530B1 Oral pharmaceutical composition containing a block copolymer The invention relates to oral pharmaceutical compositions that comprise a water miscible micelle forming block copolymer and a compound. The copolymer can be a diblock copolymer of formula AB or BA. The copolymer could also be triblock copolymer of formula ABA or BAB, or a multiblock copolymer having repeating BA or AB units of formula A(BA)n or B(AB)n, where n is an integer. The A-block may be poly(L-lactide) or poly(D-, L-, or DL-lactic acid) and the B-block a polyethylene glycol.
CN101020056A Combined application of artemisinin and its derivative and antibiotic medicine The present invention discloses the new use of available antimalarial arteannuin and its derivatives dihydro arteannuin, antiannuic methyl ether, antiannuic ethyl ether and antiannuic amber. Arteannuin and its derivatives are used through combination with antibiotic medicine to inhibit bacterial growth and enhance the antibiotic effect of available antibiotic medicine. Especially, antiannuic amber is applied in preventing and treating bacterial infection diseases except being used as antimalarial.
CN103421085A Oligopeptide used for increasing solubilities of paclitaxel or similar medicines based on paclitaxel structure The invention discloses an oligopeptide used for increasing solubilities of paclitaxel or similar medicines based on the paclitaxel structure in a manner of non-covalent supermolecule interaction, compounds of the oligopeptide and paclitaxel or similar medicines based on the paclitaxel structure, a preparation method and a method for increasing solubilities of paclitaxel or similar medicines based on the paclitaxel structure. The oligopeptide has excellent solubilization to paclitaxel. After solubilization treatment is carried out for paclitaxel by the oligopeptide, the solubility of paclitaxel in water is raised remarkably compared to the saturated solubility thereof.
US20100150895 Nutraceutical agent for attenuating the Neurodegenerative process associated with Parkinson's disease This invention describes a comprehensive nutraceutical designed to antagonize major mitigating factors to the degenerative process associated with Parkinson's disease. The formulation is comprised of a primary base of pyruvate, succinate, α-Ketoglutarate and/or oxaloacetate, niacin/NADH, fruit extracts, anthocyanins, further combined with specific macro/micronutrients, trace elements, amino acids, flavonoids and concentrated plant sources. The nutraceutical contains all natural substances that should mitigate many of the neurodegenerative processes known to be associated with PD. Mechanisms addressed are to prevent the loss of ATP/by 1-methyl-4-phenylpyridinium rotenone, scavenge hydrogen peroxide/O2.−, augment antioxidant enzymes, prevent dopamine (DA) oxidation to DA-quinone via inhibition of COX, PLA2, LOX, xanthine oxidase, tyrosinase, prevent hyperhomocysteinemia, antagonize PARP-1 apoptosis, increase blood flow, glucose and oxygen delivery to the brain, potentiate mitochondrial function, antagonize glia iNOS and MAO or its products, chelate redox-active iron, inhibit heme oxygenase-1, inhibit alpha-synuclein aggregation, augment ATP storage, mediate anti-inflammatory effects via inhibition of PDE, MAPK p38/c-Jun NH2-terminal kinase/PGE2, antagonize excitotoxicity and downregulate N-methyltransferase, all of which contribute toward PD pathology.
US20110034448 Carbonic anhydrase inhibitor sustained release intraocular drug delivery systems Biocompatible intraocular drug delivery systems include a carbonic anhydrase inhibitor therapeutic agent and a polymeric component in the form of an implant, a microparticle, a plurality of implants or microparticles, and combinations thereof. The therapeutic agent is released in a biologically active form, for example, the therapeutic agent may retain its three dimensional structure when released into an eye of a patient, or the therapeutic agent may have an altered three. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy among others.
US20100317636 Reducing the risk of chronic lung disease in infants Described herein is a method for reducing the risk of chronic lung disease in an infant suffering from respiratory distress syndrome by administering to the infant a combination of a corticosteroid having a high local to systemic anti-inflammatory activity (e.g., budesonide) and a lung surfactant.
EP0811073B1 Use of immune modulators for making medicaments ot inhibit immune responses against co-administered recombinant viruses A method of reducing immune response during gene therapy is provided which involves co-administration of the viral vector bearing a therapeutic transgene and a selected immune modulator capable of inhibiting the formation of neutralizing antibodies and/or CTL elimination of the vectors upon repeated administration.
CA2251563C Method for maintaining an existing level of body fat and/or body weight A method of maintaining an existing level of body fat or body weight in a human which comprises administering to a human desiring to maintain that existing level a safe and effective amount of conjugated linoleic acid (CLA) to maintain that level.
EP2770991A1 Orally-administered plastid expressed cholera toxin b subunit-exendin 4 as treatment for type 2 diabetes Disclosed herein are compositions and methods for treating Type II diabetes. The compositions comprise plant expressed Exendin 4. Particularly exemplified are plant derived compositions that include a CTB-EX4 conjugate that is bioencapsulated in chloroplasts.
WO2014153919A1 Use of adenosine and derivatives thereof in prevention and treatment of drug-induced liver injury Adenosine and derivatives thereof used for preventing and treating drug-induced liver injury. The derivatives are selected from adenosine monophosphate, adenosine diphosphate and adenosine triphosphate, and the drug-induced liver injury is paracetamol-induced liver injury. The administrating dosage of adenosine or derivatives thereof is 0.1 mmol/kg-5 mmol/kg, which can decrease the enzyme activity of AST and ALT in human or mammal with drug-induced liver injury, reduce the necrosis area of hepatic parenchyma cells and raise the level of glutathione.
WO2013002248A1 Phosphoric acid ester derivative The purpose of the present invention is to provide: a novel compound which has an S1P lyase inhibitory activity and can induce the reduction in the number of lymphocytes, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt as an active ingredient. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof.
CN1939479A Multi-effect herbal hair-regenerating liquor A multi-effect hair-growing herbal liquid for preventing and treating alopecia and growing hair is proportionally prepared from 10 Chinese-medicinal materials including safflower, astragalus root, Chinese angelica root, red peony root, etc. Its preparing process is also disclosed.
EP1274423A4 Medicine for treating traumatic brain injury and other neuronal disorders A medicine for treatment of neuronal disorders and traumatic brain injury is provided which comprises an effective amount of nefiracetam.
CN102119976A External preparation for treating acute inflammatory exudative skin diseases The invention relates to an external preparation for treating acute inflammatory exudative skin diseases, which is prepared from the following raw medicines in parts by weight: 2-6 parts of kuhseng, 2-4 parts of sanguisorba, 1-3 parts of gallnut, 2-5 parts of phellodendron bark, 2-5 parts of fructus kochiae, 2-5 parts of clematis root, 2-5 parts of american lopseed and 1-3 parts of dried alum. The external preparation provided by the invention can be lotion, liniment, spray or tincture and has the functions of clearing heat to eliminate dampness and gathering dampness to relieve itching after being applied to the affected parts of acute inflammatory exudative skin diseases, thus wind, heat, toxicity and dampness can be eliminated and gathered, and the effect is obvious.
CN101463062B Compound separated from Gynostemma pentaphylla total saponin acid hydrolysis products The invention discloses a compound which is separated from acid hydrolysate of the Saponins from Gynostemma pentaphylla; the structural formula of the compound is a formula, named (3beta, 23S)-3-hydroxydammar-20, 24-dien-21-oic acid 21, 23-lactone, the molecular formula is C30H46O3 and the molecular weight is 454.The evaluation by the applicant and a cell toxicant activity test prove the compound has cell toxicant activity to cancer cells in lactiferous duct (MDA-MB-435) and can be applied to preparation of antitumor drugs.
US20080108707 treating with honokiol, honokiol-type compound or magnolol, magnolol-type compound; skin disorders, cancer Pharmaceutical compositions and methods of treating conditions such as angiogenic-, neoplastic-, and cancer-related conditions and skin conditions are disclosed. The methods include administering to a host in need of treatment an effective amount of at least one honokiol-type compound and/or at least one magnolol-type compound. In addition, the pharmaceutical compositions include at least one honokiol-type compound and/or at least one magnolol-type compound in combination with a pharmaceutically acceptable carrier. The honokiol-type compound and/or magnolol-type compound are present in a dosage level effective to treat conditions listed above.
CN102579441A Application of mycoepoxydiene nicotinic acids derivatives in preparation process of pro-inflammatory mediator inhibitors The invention discloses the application of mycoepoxydiene nicotinic acids derivatives in the preparation process of pro-inflammatory mediator inhibitors, and relates to the mycoepoxydiene nicotinic acids derivatives 4-NDM (4-N Dodecyl Mercaptan). The provided application of the mycoepoxydiene nicotinic acids derivatives in the preparation process of the pro-inflammatory mediator inhibitors particularly relates to the application of the mycoepoxydiene nicotinic acids derivatives in the preparation process of drugs that are used for treating inflammatory diseases such as endotoxin shocks which are mediated by inflammatory factors. The molecular formula of the mycoepoxydiene nicotinic acids derivatives is C19H19NO4. Pharmacology experiments prove that the mycoepoxydiene nicotinic acids derivatives can effectively inhibit the expression of the inflammatory factors such as tumor necrosis factor (TNF-Alpha), interleukin 6 (IL-6) and nitric monoxide (NO). The mycoepoxydiene nicotinic acids derivatives can be used for preparing the pro-inflammatory mediator inhibitors, especially, the mycoepoxydiene nicotinic acids derivatives can be used for preparing the drugs for treating inflammatory diseases such as endotoxin shocks which are mediated by inflammatory factors.
CN101091698A New type antineoplastic medicine, and preparation method The present invention relates to an antineoplastic medicine and its preparation method. The invented antineoplastic medicine is a liposome containing mixture formed from lentinan, mitoxantrone and mitoxantrone hydrochloride according to any mixing ratio. Said invention also provides the concrete steps of its preparation method.
EP1135106B1 Sustained release matrix systems for highly soluble drugs Disclosed are sustained release oral solid dosage forms comprising a therapeutically effective amount of a medicament having a solubility of more than about 10 g/l; a pH modifying agent; and a sustained release matrix comprising a gelling agent, said gelling agent comprising a heteropolysaccharide gum and a homopolysaccharide gum capable of cross-linking said heteropolysaccharide gum when exposed to an environmental fluid, said dosage form providing a sustained release of said medicament after oral administration to human patients.
EP1551381A2 Styrylacrylonitrile compounds for inhibition of vascular endothelial growth factor This invention relates to therapeutic organic compounds and inhibition of secretion of vascular endothelial grown factor (VEGF) and its effects, including angiogenesis.
CN101705005B Method for modifying performance of compound resin by using tetrapod-like zinc oxide whiskers The invention discloses a method for modifying the performance of a compound resin by using tetrapod-like zinc oxide whiskers, which comprises the steps of: (1) mixing a compound resin filler and the tetrapod-like zinc oxide whiskers evenly to form a mixture, and adding a surface treatment liquid into the mixture for treatment to obtain an antibacterial filler, wherein the mass percentage of the tetrapod-like zinc oxide whiskers in the mixture is between 1 and 10 percent, and the balance is the compound resin filler; and (2) mixing the antibacterial filler obtained in the step(1) with a resinmatrix for solidification to form a solidified antibacterial compound resin, and finally realizing the modification of the performance of the compound resin. The antibacterial compound resin preparedby the method has the advantages of high antibacterial efficacy, good safety and stability, no discoloration, low price and the like; moreover, the tetrapod-like zinc oxide whiskers can improve the mechanical strength of the compound resin while giving the antibacterial ability to the compound resin. At present, a tetrapod-like zinc oxide whisker antibacterial agent is widely applied in industrials of antibacterial plastics, ceramics and textile, just begins to be applied in the pharmaceutical industry, and is not yet applied to dental compound resin materials.
US7700133 Antimicrobial formulations and methods of using the same Formulations and blends are described comprising zinc, silver, bismuth and copper in non-toxic amounts that are useful as treatments of a wide variety of conditions and diseases promoted by bacteria or other microorganisms.
US20080146597 Therapeutic Tetrahydroisoquinoline-Based Compositions for Cancer Therapy Disclosed are therapeutic tetrahydroisoquinoline compositions for the treatment of cancer, these compositions having selectivity for cancer cells while demonstrating few, if any, deleterious side effects on normal cells.
WO2007100822A3 Fluvastatin sodium pharmaceutical compositions Various fluvastatin compositions and methods for preparing them are described. One example is a controlled release pharmaceutical composition comprising fluvastatin and at least one non-ionic hydrophilic polymer, wherein the composition is substantially free of hydroxypropyl methylcellulose. Another example is a stable pharmaceutical composition comprising fluvastatin, preferably, fluvastatin sodium wherein the composition is substantially free of an alkalizing stabilizing agent. Another example is a stable controlled release pharmaceutical formulation, comprising fluvastatin, preferably, fluvastatin sodium, that is stable with a water content greater than 3.5 percent by weight.
CN101966158A Bendamustine hydrochloride freeze-dried powder injection for injection and preparation method thereof The invention relates to the technical field of medicinal preparations. Bendamustine hydrochloride is easy to degrade in the preparation process, so in order to prevent degradation products from generating, the aqueous solution of tertiary butanol with certain concentration is used as a solvent; therefore, medicaments and relevant auxiliary materials are dissolved, and the dissolved mixture is subjected to freeze-drying so as to obtain the bendamustine hydrochloride; however, the tertiary butanol is harmful to human bodies when inhaled or orally taken, the conventional literature indicates that the tertiary butanol can cause the oxidative injury of deoxyribonucleic acid (DNA), and experiments of rats and mice prove that the tertiary butanol has the carcinogenicity. The invention provides a bendamustine hydrochloride freeze-dried powder injection for injection and a preparation method thereof. In the preparation method, an organic solvent and particularly the tertiary butanol are not added in the processes of preparation and freeze-drying, so the safety of production and clinical medication is improved greatly. The bendamustine hydrochloride freeze-dried powder injection for the injection has the high stability and water solubility, has the characteristics of stability, controlled quality, safety and reliability, and particularly does not have organic solvent residues.
CN102697711A Desloratadine oral liquid preparation and preparation method thereof The invention discloses a desloratadine oral liquid preparation which comprises desloratadine, cyclodextrin, EDTA and water, wherein the mole ratio of desloratadine to cyclodextrin is 1:1-1:10, the concentration of desloratadine in the oral liquid preparation is 0.1mg/ml-1mg/ml, and the cyclodextrin is hydroxypropyl-beta-cyclodextrin or sulfobutyl-beta-cyclodextrin. According to the invention, cyclodextrin is added to the desloratadine oral liquid preparation prescription, the stability of the oral liquid preparation is greatly increased, and no degradation impurity is produced.
CN102940631A Application of Blebbistatin in promoting stem cell survival and keeping stem cell dry The invention relates to an application of Blebbistatin in preparing medicines, a medicine composition of Blebbistatin, a medicine for treating or preventing alopecia, a personal care composition, a stem cell medium, and an application of the stem cell medium in culturing stem cells, wherein the medicine containing Blebbistatin is used for at least one of the following purposes of promoting stem cell survival and keeping stem cell dry.
CN101574353A Antiphlogistic antibacterial paint for treating eczema dermatitis, and detection method thereof The invention discloses antiphlogistic antibacterial paint for treating eczema dermatitis, and a detection method thereof. The paint consists of adrenal cortex hormone, broad-spectrum antibiotics, antiphlogistic analgesics and drug transdermal absorption accelerator. The preparation has antiphlogistic, analgesic, antipruritic, antibacterial, antifungal and anti-allergic efficacies, and has unique effects of treating various skin inflammations, itching, allergies and bacterial/fungal infections. The paint can be used for eczema (sub-acute/chronic phase), dermatitis (seborrheic dermatitis, neurodermatitis, contact dermatitis, allergic dermatitis, insect bite dermatitis and the like), prurigo, pruritus, drug eruption, pompholyx, manus and tinea pedis, psoriasis, finger-palm keratosis, vitiligo, pityriasis rosea and the like. While studying antiphlogistic antibacterial paint, the invention also establishes a simple reliable medicine detection method for the antiphlogistic antibacterial paint. The method adopts high performance liquid chromatography and can simultaneously and accurately detect the content of three main medicaments under detection wavelength of 254 nm and other conditions.
US20100255085 Progesterone Solutions for Increased Bioavailability Fill materials for hydrophobic drugs, such as progesterone, and methods of making and using thereof are described herein. The fill material contains the hydrophobic drug dissolved in one or more fatty acids. The concentration of the hydrophobic drug is typically from about 7% to about 50% by weight of the fill material. The concentration of the one or more fatty acids is from about 60% to about 95% by weight of the carrier. The formulation also contains an organic acid and one or both of one or more pharmaceutically acceptable alcohols and one or more pharmaceutically acceptable mono-, di-, or triesters of medium or long chain fatty acids. The fill material can be encapsulated in a hard or soft capsule. The formulations described herein have a higher dissolution rate and faster onset of dissolution compared to micronized progesterone suspended in an oil and thus should have increased bioavailability in vivo.
US20050187145 template-fixed beta -hairpin peptidomimetics incorporating a template-fixed chain of 7 or 11 alpha -amino acid residues which, depending on their position in the chain, are Gly, or Pro, or of certain types; inhibitors of various serine proteases such as trypsin, human cathepsin G, and thrombin Template-fixed β-hairpin peptidomimetics of the general formulae (1), wherein Z is a template-fixed chain of 7 to 11 α-amino acid residues which, depending on their positions in the chain (counted starting formteh N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the aove formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
US20120157542 Method to assess prognosis and to predict therapeutic success in cancer by determining hormone receptor expression levels The present invention is related to a method of classifying a sample of a patient who suffers from or being at risk of developing cancer, said method comprising the steps of determining in said sample from said patient, on a non protein basis, the expression level of at least one gene encoding for a hormone receptor selected from the group comprising estrogen receptor, progesterone receptor and/or androgen receptor in said sample; comparing the one or more expression level(s) determined with one or more expression level(s) of one or more reference genes, and classifying the sample of said patient from the outcome of the comparison into one of at least two classifications.
CN103468606A Klebsiella oxytoca and application thereof in allitol production The invention discloses a new stain of Klebsiella oxytoca G4A4 CGMCC No.7662 and application thereof in allitol production, that is the screening bacterial stain of Klebsiella oxytoca G4A4 is prepared into resting cell and is used for allitol production, thereby compensating for the insufficiency of the prior art. The bacterial stain of Klebsiella oxytoca G4A4 has ribose ribitol dehydrogenase, which has a wider substrate spectrum, and under the anaerobic condition, D-psicose can be reduced to allitol. The bacterial stain of Klebsiella oxytoca G4A4 can be applied to the allitol production with D-psicose as substrate, and simple medium can be used for rapid growth and large scale enlarging culture, and the developed allitol production function of bacterial stain of Klebsiella oxytoca G4A4 has a wide application prospect.
WO2014154726A1 Biaryl-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula (I), wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
WO2014103950A1 (hydroxystilbene compound)-(sinapinic acid) reaction product having antifeeding activity An antifeeding agent characterized by comprising a reaction product of a hydroxystilbene compound with sinapinic acid (i.e., a (hydroxystilbene compound)-(sinapinic acid) reaction product) which is represented by formula (1) (wherein R1 to R4 independently represent a hydrogen atom, a hydroxy group, a saturated or unsaturated linear or branched alkoxy group having 1 to 10 carbon atoms, or a saturated or unsaturated linear or branched alkyl group having 1 to 10 carbon atoms, wherein R1 to R4 may be the same as or different from one another) or a pharmaceutically acceptable salt of the reaction product. The antifeeding agent is a novel antifeeding agent that is safe, can be ingested for a long period and has much practical application.
US20060234990 Compositions of boswellic acids derived from Boswellia serrata gum resin, for treating lymphoproliferative and autoimmune conditions A method of treatment of lymphoproliferative and autoimmune disorders with a new composition of four boswellic acids including β-boswellic acid, 3-O-acetyl-β-boswellic acid, 11-keto-β-boswellic acid, and 3-O-acetyl-11-keto-β-boswellic acid. Boswellic acids of invention have been obtained in a novel industrial process from the gum resin of Boswellia serrata tree, providing standardized composition which inhibits DNA, RNA and protein synthesis of the target cell without cytotoxic effects. The composition of invention provides advantage of irreversible cytostatic therapy, equivalent to biological effects of a cytotoxic therapy without killing body cells.
CN1679614A Medicinal composition for treating viral hepatitis, hepatocirrhosis and congestive cardiac failure A composite medicine for treating viral hepatitis, hepatocirrhosis, and congestive heart failure is prepared proportionally from 10 active components including juvabe 300, bepella, pyridoxinium hydrochloride, sodium pantothenate, etc.
WO2006059357A9 Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/ or reversing ocular diseases related with ocular neovascularization The present invention concerns the use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/ or reversing ocular diseases related with ocular neovascularization. Particularly, the above-mentioned diseases are (wet) age-related macular degeneration, (proliferative) diabetic retinopathy, neovascular glaucoma, retinal vein occlusion, or retinopathy of prematurity (ROP).
US8765376 Methods for identifying and compounds useful for increasing the functional activity and cell surface expression of CF-associated mutant cystic fibrosis transmembrane conductance regulator The present invention relates to agents, and methods for identifying compounds, which agents and compounds result in the modulation of cellular trafficking of proteins in particular that of CF-associated mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR). In addition, the invention relates to compositions and methods for the use thereof in treating conditions that are characterized by an ER-associated protein misfolding and abnormal cellular trafficking of disease-associated proteins, including cystic fibrosis (CF).
US6884808 Acids and salts such as 4-(4-(2-(2-(5,6,7,8-Tetrahydro-5,5,8, 8-tetramethylquinoxalyl))pyrrolyl))benzoic acid, used retinoic acid receptor agonists for the prophylaxis of cancer, skin disorders, asthma, alopecia or autoimmune diseases Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a —CONH— group or a group represented by the formula —CR6═CR7— in which R6 and R7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.
US20080319031 Novel Tyrosine Derivatives The present invention relates to novel tyrosine derivatives of formula (I), their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel tyrosine derivatives of the general formula (I).
US20100196448 Wound healing dressing and methods of manufacturing the same Disclosed are a hydrogel dressing for covering or treating a wound and a method for preparing the same. The hydrogel dressing includes a matrix structure of a cross-linked mixture, and an elastic sheet coated with an elementary metal or ionic metal embodied in the matrix structure. The mixture comprises a hydrophilic polymer, about 0.5 to about 5 wt % of a photocatalyst agent and at least 80 wt % of water based on the total weight of the mixture.
US20110097299 Swellable and degradable microspheres Swellable and degradable microspheres are described. The microspheres are prepared by a process that is reliable and high yielding, and makes use of a low temperature azo initiator, a small molecule chlorinated solvent as the organic phase, and a heat treatment step, and is carried out in absence of a crosslinking agent. The microsphere preparation made using the process is particularly useful as a degradable embolic material.
CN1650879A Diammonium glycyrrhizate oral cavity disintegrating agent and its preparation method An orally disintegrating tablet of diammonium glycyrrhetate is proportionally prepared from diammonium glycyrrhetate and them edical auxiliary composed of filler, disintegrant, effervescent agent, lubricant and flouring.
CN102793815A Medicament for treating soft tissue pain and tenosynovitis The invention relates to a medicament for treating soft tissue pain and tenosynovitis. The medicament is characterized by comprising the following raw materials in parts by weight: 8 to 10 parts of Chinese mugwort leaf, 10 to 15 parts of borneol, 8 to 10 parts of safflower, 10 to 15 parts of rhizoma arisaematis, 8 to 10 parts of Chinese rhubarb, and 8 to 10 parts of eucommia bark. The medicament has the advantages of short treatment course, high cure rate, no pain or wound and is convenient, comfortable and safe in use.
WO2013175357A3 Compositions and methods for treatment of inflammatory bowel disease Disclosed are compounds of Formula (I) and Formula (II) or their pharmaceutical acceptable salts. The pharmaceutical compositions comprising an effective amount of compounds of Formula (I) or Formula (II) may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used for treatment of gastrointestinal diseases and inflammation such as inflammatory bowel disease, ulcerative colitis, mild-to-moderate Crohn's disease, rheumatoid arthritis, inflammatory arthritis, psoriatic arthritis, liver cirrhosis and idiopathic urticaria.
US20090264457 Combination of at least two 5HT6-Ligands The present invention relates to a Combination of at least two 5HT6-Ligands of which one is a partial or agonist while the other is a full antagonist or an inverse agonist, a medicament comprising this comination, the use of the combiantion in the manufacture of a medicament for the treatment of memory disorders ADHD, and methods of treatment using the combination or its members.
US20110200588 Methods for genetic analysis Methods of treating an individual exhibiting a medical condition are disclosed. The methods involve determining a score of an individual based on the individual's genotypic information, comparing the score to at least one threshold value, wherein the result of the comparison is indicative of a beneficial response to a treatment, and providing a suitable treatment to the individual.
CN103211750A Method of preparing soy isoflavone nanoparticles by precipitation with compressed antisolvent (PCA) using a supercritical fluid The present invention relates to a method of preparing a solid form of soy isoflavone (e.g. genistein). In particular, the present invention relates to a method of preparing a solid form of soy isoflavone by precipitation with compressed antisolvent using a supercritical fluid to produce nano-sized particles of soy isoflavone with an improved dissolution rate and bioavailability. An oral composition or aerosolized formulation comprising the nanoparticles of the soy isoflavone prepared by the method of the present invention is also disclosed herein. The dissolution rate and bioavailability of the nanoparticles of the soy isoflavone prepared by the method of the present invention have a 2-fold increase and a 2.6-fold increase respectively as compared to those of the raw soy isoflavone.
CN103169669A Agomelatine covered pellet and drug composition capable of being dispersed in mouth The invention belongs to the fields of pharmacology and pharmaceutical engineering and relates to an agomelatine covered pellet and a drug composition capable of being dispersed in the mouth. Concretely, the agomelatine covered pellet comprises an agomelatine main drug and a polyvinylpyrrolidone binding agent. According to the invention, agomelatine covered pellets are hardly adhered, so that pellet coating efficiency is improved and the problem that a spray gun is blocked is avoided; and the agomelatine-containing drug composition capable of being dispersed in the mouth can disintegrate quickly and is good in taste and high in bioavailability. The agomelatine-containing covered pellet and the drug composition capable of being dispersed in the mouth, which are provided by the invention, are easy to prepare, cost is reduced, and the agomelatine-containing covered pellet and the drug composition capable of being dispersed in the mouth are especially applicable to industrial production.
CN101597312A Vitamin A acyl cytosine arabinoside conjugate and pharmacome thereof as well as preparation methods and application thereof The invention discloses a vitamin A acyl cytosine arabinoside conjugate with amphipathic and a pharmacome formed by the conjugate. The invention also discloses preparation methods and the application as the antitumor agent of the conjugate and the pharmacome. The invention enables RA and cytosine arabinoside 4'-amido to be coupled so as to obtain the vitamin A acyl cytosine arabinoside conjugate with amphipathic, and the conjugate has the characteristic of self assembly of the pharmacome, thereby not only protecting the cytosine arabinoside 4'-amido from devitalizing, but also enabling the conjugate and prepared pharmacome to have the tumor targeting ability. The invention respectively takes human leukaemia cells HL-60 and S180 ascites carcinoma mousse to value the antineoplastic activity of a compound of formula I and the pharmacome prepared by the compound in vivo and in vitro, and test results show that the compound of formula I and the pharmacome thereof have excellent antineoplastic activity.
CN1562051A Clarithromycin release control tablet and method for administration and production thereof A release-controllable clamycin tablet is prepared through proportionally mixing water-insoluble clamycin with filler, hydrophilic gel and adhesive, granulating, drying, dia presing, and coating.
US20120122907 Novel Pyrazole Derivatives and their use as Positive Allosteric Modulators of Metabotropic Glutamate Receptors The present invention relates to novel compounds of Formula (I), wherein M, P, X1, (A)m and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
CN103599539A Combination therapy comprising SGLT inhibitor and DPP4 inhibitor The present invention relates to combination therapy comprising a DPP4 inhibitor and an SGLT inhibitor. The combination of the present invention leads to increased plasma GLP-1 level and the combination is useful for prevention or treatment of conditions such as diabetes and diseases related to diabetes.
US20120277320 Inhibition of the survival of skin cancer by cyclohexenone compounds from antrodia camphorata The present invention relates to a novel application of a compound. The compound 4-hydroxy-2,3-dimethoxy-6-methyl-5-(3,7,11-trimethyl-dodeca-2,6,10-trienyl)-cyclohex-2-enone of the invention is isolated and purified from the extracts of Antrodia camphorata, which can be applied for inhibiting the survival of skin cancer cells and be used as a pharmaceutical composition to inhibit the skin tumor growth.
US20100209516 Triggered Drug Release Via Physiologically Responsive Polymers A drug delivery system, product and method which effectuates delivery of appropriate amounts of a pharmaceutically active agent only upon stimulus of a physiological agent released during a disease event are described. A polymer that can bind to a specific biological stimulus and respond with a specific response is included. The response may be release of a pharmaceutical agent, an optical signal or a change in physical properties of the polymer. The design of associative polymers that are held together using temporary bonds which will dissolve, break apart or swell in the presence of the specific stimulus are described. One embodiment includes a reversible response to a biological stimulus.
CN102038767A Application of effective part of Chinese dates and rutin in preparation of antilipemic drug and antilipemic drug The invention discloses an application of an effective part of Chinese dates and rutin in the preparation of an antilipemic drug and an antilipemic drug. The antilipemic drug is prepared from the antilipemic effective part of Chinese dates and rutin. The combination use of the antilipemic effective parts of Chinese dates, namely polysaccharides of Chinese dates, and rutin can obviously lower the TC (Total Cholesterol) and LDL-C (Low-Density Lipoprotein Cholesterol) levels in the serum of a mouse with hyperlipoidemia, and can obviously increase the HDL-C (High-Density Lipoprotein Cholesterol) level, wherein the dosage of the antilipemic effective parts of Chinese dates and the rutin are respectively reduced by 50%. The polysaccharides of Chinese dates and rutin have good synergistic action on the aspect of TC and LDL-C; the combination use of the polysaccharides of Chinese dates and the rutin can be used for treating IIa and IIb hyperlipoproteinemia with normal or slightly increased TG (Triglyceride) and obviously increased TC and LDL-C.
EP1545208A2 Methods of using beta glucan as a radioprotective agent The invention relates to methods for treating and preventing radiation and/or chemotherapy related injury and/or afflictions, such as myelosuppression and decreased macrophage activity, by administering a prophylactically or therapeutically effective amount of particulate, bioavailable β(1,3; 1,6) glucan. The invention also relates to methods in which β(1,3; 1,6) glucan is provided in the form of whole glucan particles, microparticulate β-glucan particles or a combination thereof.
CN102058522A Peramivir injection and preparation method thereof The invention discloses a Peramivir injection and a preparation method thereof. The Peramivir injection is composed of Peramivir, non aqueous solvent, cosolvent and water for injection, wherein the weight measurement ratio (g/ml) of the Peramivir to the non aqueous solvent is 1:(10-100), preferably 1:(15-60); the use ratio of the non aqueous solvent in a prescription is 20-60%(v/v), the use ratio of the cosolvent is 1-20% (w/v), and each injection contains 0.5 or 1.0g/ml of the Peramivir. The Peramivir injection provided by the invention is subjected to an accelerated stability test, an animal hemolysis test, an heat source examination, an irritation test and an irritability test, and all tests indicate that the Peramivir injection completely conforms to the standard. The Peramivir injection has the characteristics of stable quality, quick effect and low toxic or side effect, can be used for avoiding the problems that solvent is feculent, medicaments can not be administrated and the like when the injection is diluted to use clinically, and can satisfy the clinical requirement.
CN103479648A Application of Kadcoccitones A to in preparation of anti-platelet aggregation medicament The invention relates to an application of Kadcoccitones A to in preparation of an anti-platelet aggregation medicament. The application of the Kadcoccitones A to in the preparation of the anti-platelet aggregation medicament in the invention belongs to ais first disclosuredisclosed for the first time. The Kadcoccitones A belongs to a brand new matrix type, and has high anti-platelet aggregation activity and the characteristic of outstanding substantiality; meanwhile, the Kadcoccitones A is a significant progress in anti-platelet aggregation.
CN103435560A Synthesis and application of aceanthrylene [1,2-b] quinoxaline derivative with flexible side chain The invention relates to the technical field of biological organic synthesis, in particular to an aceanthrylene [1,2-b] quinoxaline derivative with a flexible side chain, and a preparation method and an application of the aceanthrylene [1,2-b] quinoxaline derivative. The aceanthrylene [1,2-b] quinoxaline derivative has a structure of a general formula A; the preparation method of the derivative is to increase a conjugation area of a parent and improve the water solubility of the parent by the steps of taking acenaphthequinone as a starting raw material, brominating, cyclizing and leading a flexible amine chain in; and a compound has wide anti-cancer activity, has a high inhibiting effect on the growth of multiple cancer cells of a liver cancer, a breast cancer and a human cervical cancer, and has a wide application prospect in preparing drugs for inhibiting the cancer cells.
CN103494836A Preparation method and application of composite calcium carbonate and vitamin D3 chewable tablets The invention relates to a composite calcium carbonate/vitamin D3 (vitamin D3 and beta-cyclodextrin inclusion complex) chewable tablet which is suitable for children, old people and other people who are difficult to absorb calcium sources. The composite calcium carbonate/vitamin D3 chewable tablet is prepared from raw materials of calcium carbonate/vitamin D3 and auxiliary materials, each tablet of the preparation contains 300mg of calcium carbonate and 100IU of vitamin D3 (vitamin D3 and beta-cyclodextrin inclusion complex), and the auxiliary materials are selected from a diluent, a binding agent, a wetting agent and a flavoring agent. The invention further relates to a preparation method of composite calcium carbonate/vitamin D3 tablets for children and old people. The formula and the preparation process are feasible and suitable for large-scale production, and the prepared composite calcium carbonate/vitamin D3 tablets have the advantages of good taste and sweet taste and are more suitable for children to take; furthermore, the tablets contain the vitamin D3 to enable the calcium sources to be relatively easy to be absorbed; the products have relatively good uniformity and relatively high dissolution rate. The composite calcium carbonate/vitamin D3 tablets for children, disclosed by the invention, are suitable for children, old people and people who are difficult to swallow and particularly suitable for children.
CN103230373A Dexlansoprazole freeze-drying powder for injection and preparation method thereof The invention provides a dexlansoprazole freeze-drying powder for injection and preparation method thereof, and the freeze-drying powder comprises dexlansoprazole, tromethamine and mannitol in weight ratio of 3 to 1-4 to 12-20. The preparation method comprises the following steps: dissolving tromethamine and mannitol by adding water, adjusting pH, resolving dexlansoprazole, filtering with filter membrane, charging, cooling to -45-35 DEG C at the speed of 0.8-1.2 DEG C/min, insulating and refrigerating for 2-4 hours, vacuuming to 10-20 Pa, heating to -15-5 DEG C within 1-3 hours at a uniform speed, insulating for 3-7 hours, and heating to 5-15 DEG C within 3-5 hours at a uniform speed, insulating for 2-4 hours, and then heating to 35-45 DEG C within 1-3 hours, insulating and drying for 35-45 DEG C, and then packing and warehousing after the product is detected qualified. The product prepared by the method has the advantages of low water content, good appearance, high stability and easy storage transportation.
CN1887264A Slow released compound anticancer prepn containing bendamustine The slow released compound anticancer injection containing bendamustine consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is the composition of bendamustine and bendamustine synergist selected from antitumor antibiotic and antimetabolite. The slow releasing supplementary material is polylactic acid/glycolic acid copolymer, polyethylene glycol/polylactic acid, EVAc, etc. The .suspending agent is carboxymethyl cellulose, etc. and has viscosity of 80-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent. The present invention can inhibit the growth of tumor effectively and enhance the curative effect of chemotherapy, radiotherapy and other non-operative treatment.
CA2274910C Flat medicament preparation for the application and release of buprenorphine or a pharmacologically comparable substance in the buccal cavity, and method of producing the same A solid pharmaceutical preparation, disintegratable in aqueous media, with a flat, foil-shaped, paper-shaped or wafer-shaped administration form, for application and release of active substances in the oral cavity is charac-terized by a content of buprenophine, of an active substance pharmacologically comparable to buprenorphine, or of a therapeutically suitable salt of buprenorphine or the pharmacologically comparable active substance.
EP2053393A1 Pladienolide target molecule, compound capable of binding to the target molecule, and screening method for the compound A method of measuring the binding activity of a test compound to a splicing factor 3b (SF3b), which comprises the following steps of: (a) contacting a labeled pladienolide compound and a test compound with a cell or a cell fraction; and (b) measuring the distribution of the bound labeled compound. The method enables to screen for a novel active compound capable of acting on (binding to) a pladienolide target molecule or the like.
WO2002068586A3 Hiv/fiv protease inhibitors With the help of X-ray structural analyses of drug-resistant HIV proteases and molecular modeling, a new type of inhibitor with a small P3 residue has been developed. These inhibitors are effective against HIV and its drug-resistant mutants, as well as FIV. Modification of existing HIV protease inhibitors by reducing the size of the P3 residue has the same effect. This finding provides a new strategy for the development of HIV protease inhibitors effective against the wild type and drug-resistant mutants and further supports that FIV protease is a useful model for drug-resistant HIV proteases, which often are developed through reduction in size of the binding region for the P3 group or the combined P3 and P1 groups.
CA2707280A1 Stabilized synthetic brood pheromone and race-specific ratios of components for manipulating the behavior and physiology of honey bees This invention relates to a 10-component stabilized synthetic honey bee brood pheromone and methods of stabilizing said pheromone by adding one or more antioxidants, thereby enabling the production and sustained use of commercial products based on that pheromone. The 11-component stabilized pheromone composition formed by adding the antioxidant tertiary-butyl hydroquinone to a synthetic blend of ethyl linoleate, ethyl linolenate, ethyl oleate, ethyl palmitate, ethyl stearate, methyl linoleate, methyl linolenate, methyl oleate, methyl palmitate and methyl stearate can be used in generic or race-specific ratios to manipulate the behavior and improve the performance of worker honey bees, resulting in overall increased vigor of the hive.
US7399748 Intravenous administration of a alpha -halogen- acryloyl distamycin derivative for therapy of tumors The present invention relates to an administration schedule comprising the intravenous administration of a α-halogen-acryloyl distamycin derivative, or a pharmaceutically acceptable salt thereof. The above administration allows the treatment of a variety of tumors in mammals.
WO2013129944A1 Controlled release compositions and their methods of use The present invention relates to a composition, the composition including a therapeutically effective amount of at least one active agent, and a base including, an amount of colloidal silica; at least one oil; and at least one surfactant, wherein the viscosity of the composition is below 1000 mPas at a shear rate of 100 1/s and at a temperature of 20°C.
CN103705924A Combined application of miR-1255a and tumor treating medicine The invention relates to the field of biological medicines, in particular relates to a small RNA (Ribose Nucleic Acid) molecule and a medical application thereof, provides combined application of miR-1255a and a tumor treating medicine, and particularly provides a medicine composition capable of influencing a tumor treating effect. The medicine composition comprises 1) a miR-1255a agonist of an effective dose and 2) the tumor treating medicine.
CN102372697A Substituted miazines compound The invention belongs to the technical field of medicine, particularly relates to a substituted miazines compound disclosed in a general formula (I) and clinically-acceptable salt thereof, wherein R1, R2, R3, R4, R5, Z or W is defined as in a specification. The invention also relates to a preparation method of the compounds and the application of the compounds in preparing medicines capable of treating and/ or preventing sexual dysfunctions.
US20120128767 Therapeutic calcium phosphate particles and methods of making and using same The present invention provides novel calcium phosphate nanoparticles suitable for efficient encapsulation of biologically active molecules. The invention further provides pharmaceutical compositions comprising these nanoparticles, as well as methods of making such nanoparticles and using them as carriers for therapeutic delivery of biologically active macromolecules.
EP1494658A1 Natural phenolic products and derivatives thereof for protection against neurodegenerative diseases The invention relates to the use of phenolic compounds and derivatives thereof for protection against neurodegenerative diseases, to compositions comprising these compounds, and to some novel phenolic compounds.
WO2005110431A1 Herbal product containing glucosamine Pharmaceutical compositions comprising a low dosage of glucosamine and at least one circulation-enhancing herbal product, such as Suberect Spatholobus Stem (aulis Spatholobi), Motherwort herb (Herba Leonuri), Tumeric Root Tuber (Radix Curcumae), Medicinal Cyathula Root (Radix Cyathulae), Sanchi (Radix Notoginseng), Danshen Root (Radix Salviae Miltorrhizae), Szechwan Lovage Rhizome (Rhizoma Chuanxiong), Yanhusuo (Rhizoma Corydalis), Zedoray Rhizome (Rhizoma Curcumae), Common Burreed Tuber (Rhizoma Sparganni), Peach Seed (Semen Persicae), Safflower (Flos Carthami), Gummi Olibanum, or Myrrha, are described. The aforementioned glucosamine and circulation-enhancing herbal compositions can be used to treat joint pain, arthritis, amenorrhea, dysmenorrhea, and muscle weakness.
US20080312205 Method and intermediates for the preparation of derivatives of n (1-benzhydrylazetidin-3-yl)-n-phenylmethylsulfonamide The invention relates to a novel method for the synthesis of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide.
WO2014026327A1 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof Provided are compounds according to Formula I or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
US20050159462 Elevates extracellular adenosine concentration for antiinflammatory and immunosuppressive effects; reaction of imidazole-4-carboxamide with a hydroxyalkylbenzoxazole or benzothiazole compound; 1-[4-hydroxy-1-(2-phenyl-4-benzoxazolyl)-3-pentyl]-imidazole-4-carboxamide Imidazole compounds having adenosine deaminase inhibitory activity represented by the formula (I): wherein R1 is optionally substituted aryl or optionally substituted heteroaryl, R2 is lower alkyl; R3 is hydroxy or protected hydroxy; X is O or S; and -A- is lower alkylene, its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.
US20100256100 Roll-on with high salicylic acid content The present invention relates to an assembly (1) for packaging and application of a cosmetic and/or dermatological composition, comprising a container (2) having an opening (3), an applicator element (4), mounted in such a way as to be freely rotatable, in the vicinity of said opening (3), the applicator element (4) comprising an outer surface which can be brought into fluidic communication with the inside of the container (2), characterized in that the container (2) comprises a cosmetic and/or dermatological composition in the form of a gel having a viscosity at 25° C. of between 0.1 and 60 poises, and comprising, in a physiologically acceptable medium: (a) at least 1% by weight of salicylic acid and/or at least one derivative thereof, relative to the total weight of the composition; (b) at least one polyol; and (c) at least one gelling agent.
US20100247504 Powder composition A powder composition, includes: (A) an oil-soluble antioxidant substance powder; (B) a water-soluble antioxidant substance powder; and (C) thioctic acid.
EP2455083A1 Pharmaceutical composition for dermal use comprising calcipotriol and a corticosteroid The present invention relates to a pharmaceutical composition for dermal use, said composition comprising a first pharmacologically active component A consisting of at least one vitamin D or vitamin D analogue and a second pharmacologically active component B consisting of at least one corticosteroid.
WO2005074898A3 Composition comprising (s) pantoprazole and an antibiotic for treating helicobacter pylori The present invention relates to pharmaceutical compositions comprising (s) pantoprazole and a helicobacter inhibiting antimicrobial agent, and their use in treating or preventing gastrointestinal disorders, in particular disorders caused or exacerbated by helicobacter infection and secreted gastric acid.
CN201453685U Enteric-coated capsule of piperazine ferulate The utility model relates to an enteric-coated capsule of piperazine ferulate. The enteric-coated capsule of piperazine ferulate is made of an enteric film material layer and piperazine ferulate drug preparation which is filled in the enteric film material layer. The utility model overcomes the problems of a gastric-soluble capsule of piperazine ferulate that the bioavailability is relatively low in gastric acid environment, and gastric mucosa hemorrhage can be caused by taking the gastric-soluble capsule of piperazine ferulate for a long time. The bioavailability of the enteric-coated capsule of piperazine ferulate in the alkaline environment of a small intestine (intestinal juice is alkaline) is remarkably better than that of the gastric-soluble capsule of piperazine ferulate in a gastric acid environment, so that potential hemorrhage risk is greatly reduced.
CN103520146A Application of euphoriafactor L1 in aspect of preparation of multidrug resistance reversal agent for tumors The invention belongs to the field of a biological medicine, and relates to application of euphoriafactor L1 (euphoriafactor L1, EFL1) used as a multidrug resistance reversal agent for tumors, especially relates to treatment of multidrug resistance tumors by combining with antitumor drugs, so as to restore the sensitivity of tumor cells to the anti-cancer drugs. The invention also relates to a mechanism of the euphoriafactor L1 for reversing the multidrug resistance of the tumors, namely multidrug resistance (MDR) of ABCB1-mediaed tumor cells are reversed by enhancing ATP enzymatic activity of ABCB1 in the tumor cells and inhibiting an efflux function of the ABCB1; ABCB1 expression in MDR cells in messenger ribonucleic acid (mRNA) or protein level is not reduced.
EP1763534A1 NOVEL 2-SUBSTITUTED D-HOMO-ESTRA-1,3,5(10)-TRIENES AS INHIBITORS OF 17ß-HYDROXYSTEROID DEHYDROGENASE TYPE 1 The invention relates to novel 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula (I) wherein R2 represents a C1-C8 alkyl, a C1-C8 alkyloxy group or a halogen atom, R13 represents a hydrogen atom or a methyl group, and R17 represents a hydrogen atom or a fluorine atom. The invention also relates to the pharmaceutically acceptable salts of said compounds, to the production thereof, and to the use of the same as medicaments for the prophylaxis and treatment of oestrogen-dependent diseases that can be influenced by the inhibition of 17ß-hydroxysteroid dehydrogenase type 1.
WO2008052658A1 Novel diphenylazetidinone substituted by piperazine-1-sulfonic acid having improved pharmacological properties The invention relates to the compound of the formula (I) and to its physiologically compatible salts. The compound is suitable, for example, as a hypolipidemic agent.
CN101428036A Uses of modified polysaccharide rich ingalactose in medicament for treating inflammatory bowel diseases The invention relates to the application of modified polysaccharide rich in galactose in medical preparation, in particular to application of modified polysaccharide rich in galactose in medicines for preventing and treating inflammatory bowel diseases. Aiming to fill the blank of preventing and treating inflammatory bowel disease by targeted gm-3-TLR4 access, the invention provides the technical scheme of the application of modified polysaccharide rich in galactose in treating inflammatory bowel disease, and the modified polysaccharide rich in galactose comprises natural gum or plant polysaccharide. The invention has the advantages that galectin-3 is used as the acting target, and the change of TLR4 in IBD is influenced through the regulation of the change of galectin-3, thereby promoting cell multiplication, inhibiting apoptosis and promoting injury repair. By adopting modified polysaccharide rich in galactose to treat colitis, the efficacy is good, high expression of galectin-3 can be induced, and the injury repair can be promoted; therefore, the side effect is small, and the modified polysaccharide rich in galactose can be used for a long term.
WO2008046756A1 Aminomethyl-2-imidazoles with affinity with the trace amine associated receptors The present invention relates to compounds of Formula (I) and to their pharmaceutically active salts. It has been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.
CN202859699U Cistanche decoction piece product The utility model discloses a cistanche decoction piece product. The utility model aims to solve the problem of providing a cistanche lozenge. The cistanche lozenge is composed of three layers, wherein the inner layer is a cistanche layer, while the middle layer is a tonic layer and the outer layer is a sugar coating layer. The cistanche lozenge product is a tablet prepared from the cistanche as the main raw material and additional common tonics through pressing. The cistanche lozenge is an ellipsoid or a cuboid. The cistanche lozenge prepared according to the scheme is characterized in that the cistanche is not subjected to the processes such as drying, wetting and the like in the processing procedure so that the active ingredients of the cistanche are stored to the utmost extent; therefore, the absorption and utilization of the active ingredients can be effectively realized; besides, the process is simple and convenient, and can be implemented on the original tablet production equipment; and as a result, no extra equipment cost needs to be added.
CN1631366A Enteric coated sustained releasing tablet of gliclazide óÄ and its preparation process The invention relates to an enteric coated sustained releasing tablet of gliclazide II and its preparation process, wherein the tablet is prepared from gliclazide II raw material medicament and right amount of adjuvant, the intestine-dissolvable slow release tablet provided by the invention has the advantages of insolubilization in stomach, no stimulation to stomach mucous membrane, stable release, smooth and steady blood concentration, and reduced side reaction.
WO2011014661A2 Liver x receptor agonists Compounds of formula (I) as shown in the specification. Also disclosed are methods of using one of the compounds to lower the blood cholesterol level and treat cancer, atherosclerosis, diabetes, Alzheimer's disease, and corneal arcus.
CN102000162A Regeneration liquid for changing white hair into black hair and preparation method thereof The invention provides a regeneration liquid for changing white hair into black hair and a preparation method thereof. The regeneration liquid for changing white hair into black hair is prepared by fermenting the following raw materials in parts by weight: 40 to 60 parts of fleece-flower roots, 1000 to 1500 parts of water, 10 to 30 parts of lactobacillus, 5 to 20 parts of saccharomycetes, 5 to 20 parts of photosynthetic bacteria and 40 to 60 parts of brown sugar. The preparation method comprises the following steps of: soaking the fleece-flower roots in the water for 30 to 60 hours; taking clean liquid; adding the lactobacillus, the saccharomycetes, the photosynthetic bacteria and the brown sugar to the clean liquid; and mixing and fermenting for 50 to 100 hours in a sealed condition to prepare the regeneration liquid. White hair can gradually become black hair by wiping the regeneration liquid on hair and massaging the hair everyday.
CA2807524A1 Methods and compositions for treating cancer metastasis The present invention provides methods and compositions for treating cancer metastasis by cyclohexenone compounds.
WO2014025406A1 Dental materials and method of manufacture Dental materials may be made from polyhydric phenols that are non-genotoxic and exhibit estrogenic activity less than that of bisphenol S, while exhibiting properties such as strength and flexibility comparable to those of conventional BPA-derived dental materials.
WO2004034973A3 Method of treating snoring and other obstructive breathing disorders A method of pharmaceutically managing snoring and impaired breathing is provided. This invention relates to treating snoring, sleep apnea, and other forms of sleep-disordered breathing in those with or without symptoms of or the diagnosis of gastro-intestinal reflux disease (GERD). It comprises administration of a therapeutically effective dose of Prevacid (Lansoprazole) or any other medication that can be used to treat symptoms of hyper-acidity or gastro-intestinal reflux disease (GERD). The therapeutic medication may be used alone or in combination with other pharmacologic agents or mechanical modalities including but not limited to decongestants, antihistamines or mechanical nasal toilet. It also is of benefit in improving breathing disorders that are present while awake.
CN101099846B Detumescence pain-relieving Babu plaster and preparing method The invention is concerned with a kind of cataplasma for reducing swelling and ease pain and its preparation method, relating to active constitutent and matrix. The active constitutent is made of ledebouriella root, herba schizonepetae, asarum herb, Achyranthes bidentata Bl, chuanxiong rhizome, panicled swallowwort root, Rhizoma Curcumae, Ardisia crenata L, Fordia Cauliflora Hemsl, prickly ash, burreed tuber, cassia twig, dahurian angelica root, ichnocarpus loiganthus, auckandia root, fibraurea stem, acanthopanax bark, cape jasmine, eagle ood, bornanone and mentha camphor. The matrix relates to bond, emulsifier, humectant, penetration enhancer and pH moderator. This invention also relates to the component of matrix and the preparation method of cataplasma. It uses to cure wind dampness and bone ache, traumatic injury, inflammatory process of tissue of unknown origin and parotitis ache with definite effect in rapid and without side effect.
WO2010150271A1 Process for obtaining purified pterostilbene and methods of use thereof Extraction and purification of a stilbenoid, pterostilbene to 50% to 99% purity from a botanical source by pulverising and extracting with an aqueous alcohol, filtering, chromatographing, eluting with aqueous alcohol, concentrating to a paste, redissolving the paste in aromatic solvent, column adsorption to obtain a semi-solid mass and drying. The pterostilbene is used to inhibit Histone Deacetylases and administering, optionally complexed with cyclodextrin to improve water solubility and bioavailability, to manage poly glutamine repeat disorder such as Huntington's disease, spinocerebellar ataxias, spinal and bulbar muscular atrophy and dentatorubropallidoluysian atrophy.
CN102600090A Dropping pill adopting zolpidem as major active ingredients and preparation method of dropping pill The invention relates to a dropping pill adopting zolpidem as major active ingredients and a preparation method of the dropping pill. The invention aims at providing the new preparation of zolpidem dropping pill for wide patients and medical workers, and the zolpidem dropping pill has the advantages that the disintegration is fast, the medicine bioavailability can be improved, the curative effect of the medicine is sufficiently realized, the adverse reaction is reduced, the swallow taking by children and the dosage reduction taking by old people are convenient, the carrying, the storage and the transportation are convenient, the preparation method is simple, and the dropping pill is suitable for mass production. The zolpidem and pharmacy acceptable salts or hydrates of the zolpidem are used as active ingredients, some auxiliary materials in specific types and proportions are added, and the materials are made into the dropping pill according to the conventional galenic pharmacy technology.
CA2611659A1 Method for enhancing delivery and uniformity of concentration of dietary ingredients An effervescent dietary composition for enhancing the delivery of a dietary ingredient to a human comprises dissolving an effervescent containing dietary ingredient and two ingredients capable of reacting to produce effervescence in water. Once the mixture has completely dissolved the solution is immediately ingested, and an effective amount of a dietary ingredient is absorbed. Preferably, the effervescent is in the form of a tablet which contains a dietary ingredient, and a mixture of acids, and basic salts.
US20080227762 Lupeol anti-tumor agent and uses thereof The present invention provides a method of treating melanoma comprising parenterally administering to a human a therapeutically effective amount of a parenteral composition of a Lupeol-derived anti-tumor compound.
US7696180 Antisense oligonucleotide derivative as antitumor agent; biodrugs The present invention relates to therapeutic agents for treatment of solid tumors comprising an expression-inhibiting substance (an antisense oligonucleotide derivative, a WT1 mutant gene, a WT1 mutant protein, a low molecular weight substance, and the like) against the Wilms' tumor gene (WTI).
WO2013081046A1 Extract derived from grape rachis A compound shown by the general formula (1), and an antitumor agent containing this compound as an active ingredient. (A)n1-(B)n2… (1); where n1 represents any integer of 6-20, n2 represents any integer of 1-20, A is a group shown by the general formula (2), B is a group shown by the general formula (3), R1-1-R1-3 represent -O-sugar or the like, R1-4 represents -catechin or the like, R1-5 represents -H or -OH, and R2 represents -O-sugar or the like.
US20060258703 Remedy for pruritus comprising piperidine derivative as the active ingredient It is intended to find out a novel pharmacological effect of a piperidine derivative (I). Because of having an excellent antipruritic effect, the piperidine derivative (1) is useful as a therapeutic agent for itching of any types such as eye itching, skin itching and systemic itching.
US7241468 Cooking oil, baking oil comprising sucrose fatty acid ester and triglycerides with long chain, medium chain or mixed fatty acids; nongreasy, dietetics Reduced calorie fat compositions which contain combinations of substantially non-absorbable, substantially nondigestible polyol polyesters and certain reduced calorie triglycerides that function as anti-anal leakage agents and provide textural/taste benefits are disclosed. These reduced calorie fat compositions are useful in a variety of food applications, including frying oils for salted snacks, chocolate-flavored candy bars and cooking/salad oils.
CN1903188A Application of teprenone for preparing medicine for treating and/or preventing glaucoma An application of teprenone in preparing the medicine GGA for preventing and treating glaucomas is disclosed. Its advantages are high curative effect, high safety and low cost.
CN103599070A Preparation method of temperature and fluorescence probe of lipidosome loaded with gold nanocluster and anti-cancer drug The invention relates to a preparation method of a temperature and fluorescence probe of lipidosome loaded with a gold nanocluster and an anti-cancer drug. The method comprises the following steps of: 1) preparing a near-infrared emitting fluorescent gold nanocluster through the microwave pyrolysis method in an aqueous phase way by using dithio-octanoic acid as a protective agent, chloroauric acid as a raw material and sodium borohydride as a reducing agent; 2) dissolving lecithin and cholesterol with a mixed solvent consisting of chloroform and methyl alcohol, carrying out rotary evaporation to remove the solvent to obtain a thin and dried phospholipid membrane, dissolving with gold nanocluster turbid liquid and an anti-cancer drug aqueous solution, and then incubating by the supercritical carbon dioxide method to prepare lipidosome turbid liquid with the gold nanocluster and the anti-cancer drug loaded in an inner water phase. Compared with the prior art, the method has the advantages of being simple and relatively low in cost; the prepared lipidosome drug carrier has light-induced heat sensitivity and fluorescence intensity heat sensitivity, and a novel temperature and fluorescence probe on the basis of the lipidosome drug carrier can be developed, so that important reference value is brought for preparation and application of other drug carriers.
CN101773487A Exotic plant Flaveria bidentis active ingredient chlorogenic acid intercalation hydrotalcite and preparation method thereof The invention discloses an exotic plant Flaveria bidentis active ingredient chlorogenic acid intercalation hydrotalcite and a preparation method thereof, belonging to the field of pesticide or medicine. The structural formula of the exotic plant Flaveria bidentis active ingredient chlorogenic acid intercalation hydrotalcite is M2+1-xM3+x(OH)2(C16H18O9)x.mH2O. Exotic plant Flaveria bidentis active ingredient chlorogenic acid is separated by countercurrent chromatography process, NO3- between laminates of precursor hydrotalcite is substituted in reaction by utilizing ion exchange process to construct anion type supermolecule laminated material. The invention has the following advantages: exotic plant Flaveria bidentis active ingredient chlorogenic acid having pesticide or medicine properties is put between hydrotalcite laminates to realize effective storage of exotic plant Flaveria bidentis active ingredient by hydrotalcite, thus realizing slow release performance of hydrotalcite on the ingredient, and providing a new method of applying hydrotalcite to store and release exotic plant Flaveria bidentis active ingredient.
CN101066981B Non-cyclic nucleoside phosphonate compound and its composition, prepn process and use The present invention provides one kind of non-cyclic nucleoside phosphonate compounds with the general formula as shown and their pharmaceutically acceptable inorganic and organic salts and composition. The present invention also provides the preparation process of these compounds and their use as active matter for treating viral infectious diseases, especially infectious diseases caused by HBV and HIV.
EP1745789A1 Compositions comprising ribose for increasing energy in vivo Precursors of adenosine triphosphate are administered orally to increase intracellular ATP concentration as dietary supplements or for treatment of reduced energy availability resulting from strenuous physical activity, illness or trauma. Pentose sugars are administered individually, mixed into dry food or in solution. The preferred pentose is D-ribose, singly or combined with creatine, pyruvate, L-carnitine and/or vasodilating agents. Additionally, magnesium, electrolytes, fatty acids and hexose sugars can be used. The compositions and methods of this invention are especially beneficial to mammals having reduced energy availability or high energy demand.
WO2012162339A1 Use of teriflunomide for reducing occurrence of relapses requiring healthcare resources The present invention relates to the use of teriflunomide for reducing occurrence of relapses requiring healthcare resources in patients having multiple sclerosis.
CN101023969A Hippophate flavone powder capsule and its preparing method The present invention discloses a hippophae rhmnoides flavone soft capsule and its preparation method. The invented hippophae rhmnoides flavone soft capsule is formed from two portions of content material and capsule shell. Its content material is composed of hippophae rhmnoides flavone, vegetable oil and bee's wax, and its capsule shell is made up by using gelatin, water, glycerine and preserving agent. Said hippophae rhmnoides flavone soft capsule can obtain good therapeutic effect for curing the diseases of hypertension, hyperlipemia, coronary heart disease and other angiocardipathy and cerebrovascular disease.
CA2335353C Compositions comprising phenylaminothiophenacetic acid derivatives for the treatment of acute or adult respiratory distress syndrome (ards) and infant respiratory distress syndrome (irds) Novel compositions for the treatment of IRDS and ARDS are indicated which contain a compound of formula (I), in which R1 is hydrogen or 2-(2-hydroxyethoxy)ethyl and/or a pharmacologically tolerable salt of this compound and lung surfactant.
WO2009007390A3 2-pyraz inylbenz imidazole derivatives as receptor tyrosine kinase inhibitors The invention concerns pyrazine derivatives of Formula (I) or a pharmaceutically-acceptable salt thereof, wherein each of G1, G2, R1, m, R2, R3, n and R4 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
WO2010144664A1 Thiophenes as glucagon receptor antagonists, compositions, and methods for their use The present invention relates to compounds of the general formula (I): wherein R1, R2, R3, R5, s, and Z are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
US7045315 Methods for modulating expression of exogenous genes in mammalian systems In accordance with the present invention, there are provided various methods for modulating the expression of an exogenous gene in an isolated cell and in a mammalian subject employing modified ecdysone receptors. Also provided are modified ecdysone receptors, as well as homomeric and heterodimeric receptors containing same, nucleic acids encoding invention modified ecdysone receptors, modified hormone response elements, gene transfer vectors, recombinant cells, and transgenic animals containing nucleic acids encoding invention modified ecdysone receptor.
US7678760 Inhibitors of Memapsin 2 and use thereof Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1). The inhibition constant of OM99-2 is 1.6×10−9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bound to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.
WO2014100733A1 Methods and materials for treating calcific aortic valve stenosis This document provides methods and materials involved in treating cardiovascular conditions such as calcific aortic valve stenosis. For example, methods and materials for using sGC agonists or a combination of sGC agonists and PDE5A inhibitors to reduce calcification of heart valves and/or vessels or to slow progression of aortic sclerosis to calcific aortic valve stenosis are provided.
CN103690485A Oral proliposome containing atorvastatin calcium and preparation method of oral proliposome The invention relates to an oral proliposome containing atorvastatin calcium and a preparation method of the oral proliposome. The oral proliposome comprises the following components: 0.5%-10% of the atorvastatin calcium, 10%-30% of phospholipid, 2%-10% of poloxamer, 50%-87.3% of absolute ethanol and 0.2%-3% of a stabilizer. The preparation method comprises the following steps: adding the atorvastatin calcium, the phospholipid, the poloxamer and the stabilizer into the absolute ethanol solvent, mixing in the absence of water, and dissolving the mixture into a clear anhydrous solution so as to obtain an atorvastatin calcium proliposome preparation. The proliposome can be quickly self-assembled into the medicated proliposome preparation with a proper particle size and high encapsulation efficiency after being diluted by a proper hydration medium before use and is used for oral administration, the operation is easy and convenient, and the oral administration mode can be easily accepted by patients.
EP1878723A1 N-[(1,5-diphenyl-1H-pyrazol-3-yl)methyl]sulfonamide derivatives antagonists of the CB1 cannabinoids receptors Pyrazole compounds (I) in the basic or acid additive salt form, hydrate or solvate forms, are new. Pyrazole compounds of formula (I) in the basic or acid additive salt form, hydrate or solvate forms, are new. R 11-12C alkyl (optionally substituted by F, OH, 1-4C alkoxy, 1-4C alkylthio, phenoxy, -O-CF 3, -OCHF 2, -S-CHF 2, -SCF 3), T, methyl (optionally substituted by T), benzyl/benzhydryl/benzydrylmet hyl (optionally substituted by halo, OH, methylenedioxy, CN, NO 2, 1-4C alkylcarbonyl or Alk, O-Alk, S(O) n-Alk or OS(O) nAlk), phenyl (substituted by a heterocyclic radical such as pyrrolyl, imidazolyl, pyridyl or pyrrazolyl (all optionally substituted by halo or 1-4C alkyl), phenyl/phenoxy (where phenyl group is optionally substituted by halo, OH, methylenedioxy, CN, NO 2, 1-4C alkylcarbonyl or -Alk, O-Alk, S(O) n-Alk or OS(O) n-Alk) and optionally substituted by halo, OH, methylenedioxy, CN, NO 2, 1-4C alkylcarbonyl or Alk, O-Alk, S(O) nAlk or OS(O) n-Alk), T 1, tetrahydronaphthalenyl/naphthyl (optionally substituted by halo, 1-4C alkyl, di(1-4C)alkylamino or CF 3) or 2,3-dihydrobenzofuran-yl (optionally substituted by 1-4C alkyl, indol-2-yl or N-methylindol-2-yl); T : 3-12C non-aromatic carbocyclic radical (optionally substituted by 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, F, OH, CF 3, -CHF 2, -O-CF 3, -O-CHF 2, -S-CF 3 or -S-CHF 2); T 1thienyl, furyl, oxazolyl, thiazolyl, imidazolyl, pyrrolyl, pyridyl (all optionally substituted by the halo, 1-4C alkyl or CF 3); R 2H, 1-4C alkyl or 1-4C alkylsulfonyl; R 3CN, OH, 1-4C alkoxy, cyanomethyl, hydroxymethyl, 1-4C alkoxymethyl, fluoromethyl, tetrazolylmethyl, N-(methyl)tetrazolylmethyl, tetrazolyl, N-(methyl)tetrazolyl, CONR 6R 7, -CH 2S(O) n(1-4C)alkyl, -COOR 8 or CH 2NR 6R 7; R 4, R 5phenyl (optionally substituted by halo, 1-7C alkyl (optionally substituted by F, OAlk, S(O) nAlk or OS(O) nAlk)); either R 6, R 7H or 1-4C alkyl; or NR 6R 7heterocyclic radical such as pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl (optionally substituted by 1-4C alkyl); R 81-4C alkyl; n : 0-2; and Alk : 1-4C alkyl (optionally substituted by F). Independent claims are included for: (1) preparation of (I); and (2) drug, comprising (I). [Image] - ACTIVITY : Neuroleptic; Antiaddictive; Nootropic; Tranquilizer; Neuroprotective; Metabolic; Anorectic; Antidiabetic; Antilipemic; Analgesic; Gastrointestinal-Gen; Antiemetic; Antidiarrheic; Antiulcer; Hepatotropic; Immunomodulator; Antiarthritic; Antirheumatic; Antiinflammatory; Antiparkinsonian. - MECHANISM OF ACTION : Cannabinoid (CB1) receptor antagonist.
US20100069476 Compositions and methods for reduction of cutaneous photoageing Compositions and methods are provided in which a topical hydrophilic formulation includes a catechin and a hydrophilic antioxidant in a hydrophilic composition at a ratio of between 2.3 to 1.7 (by weight), ad wherein the catechin and the antioxidant are present in an amount such that application of the composition to skin will deposit the catechin at a dosage of between 0.7 mg/cm2 and 1.3 mg/cm2. Especially preferred catechins include green tea catechins, and particularly EGCG, while preferred antioxidants include ascorbic acid and derivatives thereof.
CN101724044A Human epididymis expression sperm binding protein HEL-97, encoding gene and application thereof The invention belongs to the field of biotechnology and medicine, and discloses a new human epididymis specific expression sperm binding protein HEL-97 as well as preparation and application thereof. The invention discloses an amino acid sequence of the HEL-97 protein and provides a recombination expression carrier carrying the DNA sequence for encoding the protein. The protein is located in the middle rear and tail parts of the head of a mature sperm. A RT-PCR result shows that the gene is weakly or rarely expressed in the head and tail part of the epididymis and other tissues of testis, heart, liver, spleen, kidney and stomach. A band of about 28 KD is detected in the corpus epididymidis part with Western blot. The HEL-97 protein can be used as a target protein for researching and developing immunity contraceptive as well as clinical diagnosis and treatment for male sterility. A method for detecting a corresponding gene or protein based on development of the HEL-97 protein can be widely used for the research field of reproductive medicine.
WO2013166218A1 Deactivation of urushiol and method of treatment and prevention of contact dermatitis The invention herein disclosed provides for compositions, methods for synthesizing said compositions, and methods for using said compositions, wherein the compositions and methods may be used to bind to and/or deactivate a poison oak oil, such as urushiol. The compositions and methods can be used to treat and/or reduce an inflammatory reaction and/or hypersensitivity to natural compounds found in poison oak, poison ivy, poison sumac, mango, lac tree, cashew nut, and Asian lacquer.
CN103356648A Application of Chukrasone A in preparing erythrocyte rising medicines The invention relates to a novel use of a compound Chukrasone A in the pharmaceutical field, and in particular relates to an application of Chukrasone A in preparing medicines for treating low erythrocyte. The use of the Chukrasone A in preparing erythrocyte rising provided by the invention is disclosed for the first time. As the framework type belongs to a brand-new framework type, and the inhibitory activity of the Chukrasone A to low erythrocyte is unimaginably strong, the probability of giving any enlightenment by other compounds does not exist. The Chukrasone A has remarkable substantial characteristics and meanwhile has remarkable progress for preventing and treating low erythrocyte.
CN102626420A Mixed preparation containing strontium, calcium and vitamin D The invention discloses a mixed preparation containing strontium, calcium and vitamin D. The mixed preparation comprises strontium ranelate, calcium and vitamin D. According to the technical scheme, a patient takes an effective dose of strontium, so that the development of bones and the formation of osteoid are facilitated, the generation of osteoclasts is inhibited, calcium metabolism is adjusted, an effective dose of calcium and vitamin D is supplemented, and great convenience is brought to administration of the patient.
US20080025950 Modified Macromolescules and Associated Methods of Synthesis and Use Described herein are compounds such as macromolecules that have been modified in order to facilitate crosslinking by introduction of at least one hydrazide-reactive group and/or aminooxy-reactive group, and methods of making and using thereof for scar-free wound healing, for delivering bioactive agents or living cells, for preventing adhesion after a surgical procedure or for bone and cartilage repair. The macromolecule can be an oligonucleotide, a necleic acid, a polypeptide, a lipid, a glycoprotein, a glycolipid, a polysaccharide, a protein or a synthetic polymer, preferably a glycosaminoglycan like hyaluronan.
CN103494999A Pharmaceutical composition and pharmaceutical preparation, preparation method thereof and application thereof The invention discloses a pharmaceutical composition which is characterized by comprising the following raw materials: a deer product, frankincense, myrrh, teasel root, dragon's blood, safflower, Chinese angelica, rhizoma drynariae, wolfberry, eucommia, hematoxylon, woodlouse, native copper, pseudo-ginseng, cucumber seed and nux vomica; and when 100 parts by weight of the deer product is taken as a reference, the pharmaceutical composition respectively comprises 100-200 parts by weight of the frankincense, the myrrh, the teasel root, the dragon's blood, the safflower, the Chinese angelica, the rhizoma drynariae, the wolfberry and the eucommia, 50-150 parts by weight of the hematoxylon, the woodlouse, the native copper and the pseudo-ginseng, 150-250 parts by weight of the cucumber seed, and 20-60 parts by weight of the nux vomica. The pharmaceutical composition and/or the pharmaceutical preparation is/are used when a fracture patient is routinely treated, and can effectively relieve swelling and pains, promote porosis and shorten the rehabilitation time of the fracture patient.
WO2013039428A3 Quinoline derivatives and method for producing and using same The present invention relates to novel quinoline derivatives, such as substituted 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1- phenylbutan-2-ols, to a method for producing same, and also to the use thereof as antimycobacterial agents, in particular to 5,6,7-substituted 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1- phenylbutan-2-ols of general formula (I), where R1 is Н or methoxy, R2 is Н, methoxy or -O-(CH2)n-O-, R3 is Н, methoxy or -O-(CH2)n-O-, n=1-2, and also to the pharmaceutically acceptable salts thereof with acids which exhibit activity in relation to mycobacteria. The invention also relates to a method for producing compounds of formula (I), which consists in interacting corresponding arylquinolines with an aromatic ketone and using said compounds as an active principle in the creation of anti-tubercular medicinal preparations.
WO2012065139A3 Entpd5 inhibitors The invention provides methods and pharmaceutical compositions for treating cancer or promoting apoptosis of cancer cells, or reducing the resistance of cancer cells to chemotherapy or apoptosis-promoting therapies by contacting the cancer cells with an ENTPD5-specific inhibitor.
US20100233104 Amino-Acid Functional Siloxanes, Methods Of Preparation and Applications A method of preparing an amino acid functional siloxane by reacting an amino acid derivative selected from the group of an N-acyl amino acid and an N-aroyl amino acid with an amino functional siloxane optionally in the presence of a solvent. The invention extends to personal care products containing the resulting amino acid functional siloxanes.
EP1060180B1 Process for synthesizing carbapenem antibiotics A process for the direct crystallization of a compound of formula (I) or a pharmaceutically acceptable salt thereof, is disclosed, wherein R?1 and R2¿ represent H, C¿1-10? alkyl, aryl or heteroaryl, or substituted C1-10 alkyl, aryl or heteroaryl and X?+¿ represents a charge balancing group, comprising extracting a solution containing a crude compound of formula (I) or (Ia) or a pharmaceutically acceptable salt thereof, wherein each X+ is a charge balancing group, and R?1 and R2¿ are as described above with a C¿4-10? alcohol, collecting and crystallizing the resulting aqueous phase to produce a crystalline compound of formula (I).
EP0863896B1 Novel imidazole derivatives, method for preparing same, pharmaceutical compositions and use of said derivatives as endothelin antagonists Novel compounds of formula (I), wherein R1 is alkyl, A is a sulphur or oxygen atom, R2 is carboxy, tetrazolyl or alkyl, alkoxy and alkylthio substituted by carboxy or tetrazolyl, Hal1 is halogen, q is an integer from 0 to 4, R3 is formyl, carboxy or tetrazolyl, Y is phenyl substituted by a dioxol radical and optionally by a halogen atom, or by an alkyl or alkoxy radical, and all possible isomeric, i.e. racemic, enantiomeric and diastereoisomeric forms thereof, as well as addition salts of said compounds of formula (I), are disclosed.
US20090069325 Piperidine Derivatives Useful as Modulators of Chemokine Receptor Activity The present invention relates to the compounds of formula (I): in which: and the remaining variables are defined herein. The present invention also relates to a process for preparing such compounds and use of such compounds in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
US20050080069 comprises Potassium tetrachloroplatinate and lignohumic acid ammonium salts; nontoxic An anticancer agent containing platinum preparation, humic substances, water and sodium chloride. Potassium tetrachloroplatinate is used as a platinum compound and lignohumic acid ammonium salts are used as humic substances taken in the following ratio of components per 1 ml of solution: lignohumic acid ammonium salts 0.18-0.22 mg potassium tetrachloroplatinate 0.020-0.040 mg sodium chloride isotonic solution 0.97-0.99 ml distilled water up to 1.0 ml
CN102488662A Preparation methods of ibuprofen arginine powder injection for injection The invention relates to preparation methods of ibuprofen arginine powder injection for injection, relating to preparation methods of ibuprofen arginine powder injection, which are used for solving the problems of being complex, high in cost and high in quality control difficulty in the traditional ibuprofen preparation method. The first method comprises the following steps of: mixing ibuprofen and arginine, and adding the mixture into purified water to be stirred till the mixture is completely dissolved so as to obtain a solution; carrying out ultra-filtration of the solution under a sterile environment, and split charging in a sterile manner; and freezing and drying to obtain white frozen powder, namely the ibuprofen arginine powder injection for injection. The second method comprises the following steps of: after dissolving the arginine into the purified water, adding the ibuprofen to obtain a solution; carrying out ultra-filtration of the solution under a sterile environment, and split charging in a sterile manner; and freezing and drying to obtain white frozen powder, namely the ibuprofen arginine powder injection for injection. Recovery, separation and crystallization of a solvent are not required. The methods disclosed by the invention are simple in process, low in cost, free from solvent residual, high in product yield and easy for quality control, wherein the product yield can be up to 93.1-95.8%.
CA2378487C Antibiotic(s)-polymer combination The present invention relates to an antibiotic(s)-polymer combination, which under physiological conditions guarantees the continuous release of antibiotics over a period of several days and can be used in human and veterinary medicine. The invented antibiotic(s)--polymer combination is characterized by the fact that in a homogeneous polymer mixture, consisting of one or more hydrophobic polymers from the groups of poly(methacrylic acid esters), the poly(acrylic acid esters) and the poly(methacrylic acid ester-co- acrylic acid esters) and one or more hydrophilic polymers from the group of polyethers, one or more slightly water--soluble antibiotics from the groups of aminoglycoside antibiotics, the lincosamide antibiotics, the tetracycline antibiotics and quinolone antibiotics, possibly an easily water- soluble antibiotic from the groups of aminoglycoside antibiotics, the lincosamide antibiotics and the tetracycline antibiotics, and possibly one or more organic adjuvants are suspended, and that this suspension forms a composite.
WO2011066542A2 6-substituted estradiol derivatives and methods of use Disclosed are compounds of the formula (I): where in R1, R2, R3 and R4 are independent l y hydrogen, C1 -C6 alkyl, halo, a sulfate, a glucuronide, -OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, N ( CH2 ) n; a phosphate group, and a phosphinate group; R9 is hydrogen, halogen or alkyl; R11 i s selected from the group consisting of H, C1 -C6 alkyl, halogen, a sulfate, a glucoronide, - SO2NH2, -COOH, -CN, -CH2CN-, -NHCN-, -CHO, =CHOCH3, -COO salt, -0S02alkyl, -NH2, and -NHCO ( CH2 ) n; R12 is selected from the group consisting o f H, a C1 -C6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X i s selected from the group consisting of C1 -C12 alkyl, C2 -C12 alkenyl, C2 -C12 alkynyl, halogen, a glucoronide, -NH2, - SO2NH2, -COOH, -CN, -CH2CN, -NHCN, -CHO, -COOsalt, -0S02alkyl, - SH, - SCH3, -CH [ ( CH2 ) nCH3 ] COOCH3, - ( CH2 ) mCOOCH3, - ( CH2 U-O-CH3, - ( CH2 ) m-0- ( CH2 ) nCH3, ( CH2 ) m- S -CH3, - ( CH2 U- S - ( CH2 ) nCH3, - ( CH2 ) m-NH- ( CH2 ) nCH3, -C2 -C8 alkenyl -0- ( CH2 ) nCH3, - C2 -C8 alkenyl - S - ( CH2 ) nCH3, -C2 -C8 alkenyl -N- ( CH2 ) nCH3, -C2 -C8 alkynyl -O- ( CH2 ) nCH3, -C2 -C8 alkynyl - S - ( CH2 ) nCH3, -C2 -C8 alkynyl -N- ( CH2 ) nCH3, - ( CH2 U-OH, - ( CH2 ) m-O-NH2, - ( CH2 ) m- S -NH2 , -NH ( CH2 ) mCH3, -NH ( CH2 ) mOCH3, -NH ( CH2 ) mCHOH-COOH, -N ( CH3 ) 2, - ( CH2 ) m (NH ) CH2OH, -NHCOOH, - ( CH2 ) mNHCOOH, -NO2, - SCN, - S02alkyl, -B ( OH ) 2, - ( CH2 ) m N ( CH3 ) - SO2 -NH3, - ( CH2 ) m-NH- SO2 -NH2,-NHC ( = S) CH3, and -NHNH2; and Y is selected from hydrogen, =0, -OCO(R6) and -OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and the Λ/WV symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds. The compounds are useful in the treatment of various types of cancer.
CN1788733A Gel agent containing centella general glycoside and sodium hyaluronate, its preparation method and uses The present invention belongs to the field of medicine preparation technology, and is one kind of gel preparation containing asiaticoside and sodium hyaluronate. The gel preparation can speed the formation of granulation tissue in the wound, promote the healing of wound, and form transparent and ventilate film to protect the wound tissue owing to the excellent filming property of sodium hyaluronate. The present invention also provides the preparation process of the gel preparation.
US20110159017 Trytophan catabolism in cancer treatment and diagnosis The unexpected expression of tryptophan 2,3-dioxygenase (TDO2) in cancer cells and tumors has been established. Methods for diagnosing cancer based on the expression of TDO2 are provided, as are methods for treating cancer and inhibiting the growth of cancer cells by inhibiting TDO2, as well as pharmaceutical compositions.
CN103102383A Crystal form A of glycyrrhetinic acid-30-amide derivative and preparation method thereof The invention provides a crystal form compound of N-[(3-o-chlorophenyl-isoxazol-5-yl)methyl]-11-desoxy-glycyrrhetinamide, namely a crystal form A. The invention also provides a method for preparing the crystal form A. The invention also provides a pharmaceutical composition containing the crystal form used as an active ingredient. The invention simultaneously provides application of the crystal form in the preparation of adrenal cortical hormone replacement medicaments, such as anti-inflammation, anti-allergy and the like. The crystal form can be also used for the preparation of liver protection medicaments, antiviral medicaments and the like.
CN103221051A IBAT inhibitors for treatment of metabolic disorders and related conditions The present invention regards certain IBAT inhibitors for the prophylaxis or treatment of a metabolic syndrome, obesity, a disorder of fatty acid metabolism, a glucose utilization disorder, or a disorder in which insulin resistance is involved such as diabetes mellitus type 1 or type 2 diabetes.
CN103110699A Scraping therapy oil The invention discloses a scraping therapy oil. The scraping therapy oil is composed of menthol, clove oil, eucalyptus oil, thyme oil, tea tree oil, camphor and methyl salicylate. The scraping therapy oil adopting purely natural extracted plant extract oils has the characteristics of refreshing and exciting rich fragrance, scientific component ratio, rapid skin penetration, dredging and conditioning, and uncomfortable feeling alleviating. The scraping therapy oil is used for the positions comprising epidermis, muscles, extremities joints, cervical vertebra, shoulders, thoracic vertebra, lumbar vertebra and the like, and the function obstruction involved positions caused by bump, drawing, hitting or violent motions, can improve the joint and ligament mobility, and can be used for daily healthcare or the scraping therapy.
EP2382215A1 Derivatives of 2-pyridin-2-yl-pyrazol-3(2h)-one, preparation and therapeutic use thereof The invention relates to compounds with the formula (I), in a basic state or as an acid addition salt: (I) where n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X is a -CH2, -CH(R')-, -NH(R')- group or a heteroatom selected from among O and S, where R' is a -(C1 -C5)alkyl, -(C1-C5)alcoxy, -CH2-aryl, -C(O)R5 or -COOR5 group; R1 is an oxo, -COOR5, -W-OH or -W-NR5R6 group; R2 is an H atom or a group selected from among the following groups: (i) -(C1 -C5)alkyl, (ii) -(C1-C5)alcoxy, (iii) -COOR5, (iv) -NR5R6, (v) -C(O)-NR5R6, (vi) -SO2-N R3R4, (vii) heteroaryl optionally substituted by a -(C1-C5)alkyl group, (viii) -W-aryl, (ix) -W-heteroaryl, (x) -O-W-aryl, (xi) -O-W-heteroaryl and (xii) -O-W-NR5R6; where R3 and R4, which may be identical or different, (i) independently from one another are an H atom, a -(C1-C5)alkyl, -(C3-C6)cycloalkyl, aryl, heteroaryl, -CH2-heteroaryl, -(C1-C5)alkyl-NR5R6, -W-OH or -W-NR5R6 group; or (ii) together with the nitrogen atom that carries them, jointly form a heterocycloalkyl group, optionally substituted by one or more groups selected from among the -(C1-C5)alkyl and -CH2-aryl groups; W is a -(C1-C5)alkylene group, optionally substituted by one or more hydroxy groups; R5 and R6, which may be identical or different, independently from one another are a hydrogen atom or a group selected among the -(C1-C5)alkyl groups and the -(C3-C6)cycloalkyl groups, as well as to the preparation method and to the therapeutic uses of said compounds.
US20100273737 Supplementary food composition for reducing body odor A food supplement for reducing body odor which includes a mixture of edible carriers with chitin aqueous solution lyophilized powder, chitosan aqueous solution lyophilized powder, chitin powder, chitosan powder, or a combination of these ingredients, in the form of tablets or pills. The food supplement has the outstanding effect of reducing various types of body odors, including Koreans' unique body odor, such as Kimchi smell or garlic smell; westerners' unique body odor, such as cheese smell or butter smell, Arabs' unique body odor, such as mutton smell, armpit odor and body odor that is unique to the aged.
EP1751096A2 Salt of 4- or 5- aminosalicylic acid The present invention provides L-arginine salts of 4-ammosalicylic acid and 5-ammosalicylic acid (mesalamine) Pharmaceutical compositions containing these L-argmme salts are useful for the treatment of inflammatory conditions of the gastrointestinal (GI) tract such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) The compositions may be used to treat Crohn's disease, gastritis, celiac disease, peptic ulcer disease, inflammatory conditions of the mouth and esophagus, pre-cancerous lesions of the stomach, non-ulcer dyspepsia, bacterial overgrowth, peptic ulcer disease, fissures of the intestine, ulcerative colitis, infectious colitis, precancerous conditions of the colon, proctitis, inflammation associated with hemorrhoids, protalgia fugax, rectal fissures, and liver gallbladder and/or bilary tract conditions.
US20100035858 Novel Compositions and Methods for Binding and Inhibiting 5-HT4 Receptor The present invention relates to compositions that bind to 5-HT4 receptors and inhibit proliferation of activated lymphocytes. The invention also provides methods for inhibiting proliferation and inducing cell death in activated immune cells, as well methods for treating diseases associated with activated immune cells by administering 5-HT4 receptor ligands.
EP1911446A2 The use of PPAR-gamma agonists for treating diseases characterised by neuron degeneration, neuron injury or impaired plasticity A method for the promotion of growth and/or repair of neurons in diseases or conditions characterised by neuron degeneration , injury or impaired plasticity which method comprises the administration of an effective, non-toxic and pharmaceutically acceptable amount of a PPARγ agonist or a pharmaceutically acceptable derivative thereof.
WO2010049451A2 C-glycosidic analogues of alpha-galactosylceramids having immunostimulating and immunoregulating properties The invention relates to C-glycosidic analogues of alpha-galactosylceramids of the general formula (I) having immunostimulating and immunoregulating properties.
CN102617745A Preparation method and blood sugar lowering function of Ganoderma lucidum karst polysaccharide F31 The invention discloses a preparation method and a blood sugar lowering function of Ganoderma lucidum karst polysaccharide F31. The preparation method of Ganoderma lucidum karst polysaccharide F31 comprises the steps: crushing Ganoderma lucidum karst karst fruit body, extracting with hot water, filtering, adding ethanol to filtrate for precipitating, and separating precipitate; loading the precipitate to a DEAE (2-diethylaminoethanol) sepharose fast flow chromatographic column, balancing with Tris-HCl (10mM, pH=8.0), eluting with Tris-HCl (10mM, pH=8.0) containing 0.1M NaCl, and finally eluting with Tris-HCl (10mM, pH=8.0) containing 0.5M NaCl to respectively obtain fractions F1, F2 and F3; and loading the fraction F3 to a molecular sieve Sephacryl S300, balancing with H2O, eluting with H2O, collecting effective peak, concentrating under reduced pressure, dialyzing, and drying to obtain the Ganoderma lucidum karst polysaccharide F31. According to the invention, a new Ganoderma lucidum karst polysaccharide F31 is separated from the Ganoderma lucidum karst fruit body; and the Ganoderma lucidum karst polysaccharide F31 has activity of lowering blood sugar, and can be used for preparing a medicament for treating diabetes, particularly a medicament for treating type-II diabetes, thereby laying a foundation for developing the new drugs for treating diabetes, and positively pushing the research and development of active ingredients of the natural drugs of diabetes.
CN1839850A Dispersion tablet medicine containing oryzanol and its preparation method The invention relates to a dispersible tablet containing oryzanol for treating neurological system diseases and its preparing process, wherein the tablet comprises (by weight parts): oryzanol 5-200, filling agent 20-200, crumbling agent 15-40, bonding agent 1-70, flowing adjuvant or lubricating agent 0-5.
US20130059827 Intranasal 0.6% and 0.72% testosterone gel formulations and use thereof for treating anorgasmia or hypoactive sexual desire disorder The present invention relates to lower dosage strength pernasal testosterone gel formulations for intranasal administration and treatment methods for using the lower dosage strength pernasal testosterone gel formulations for treating a female subject with anorgasmia and/or hypoactive sexual desire disorder.
US20100113567 Recombinant VSV For The Treatment of Tumor Cells The present invention relates to compositions and methods for the treatment of tumor and/or malignant and/or cancerous cells. The present invention provides VSV vectors comprising nucleic acid encoding a cytokine, such as interleukin or interferon, or a suicide gene, such as thymidine kinase, or other biological protein, such as heat shock protein gp96, or endostatin or angiostatin, wherein said VSV vectors exhibit greater oncolytic activity against the tumor and/or malignant and/or cancerous cell than a wild-type VSV vector. The present invention also provides methods of making such vectors, host cells, expression systems, and compositions comprising such VSV vectors, and viral particles comprising such VSV vectors. The present invention also provides methods for producing oncolytic activity in a tumor and/or malignant and/or cancerous cell comprising contacting said cell with a VSV vector of the present invention. The present invention also provides methods for suppressing tumor growth comprising contacting said tumor with a VSV vector of the present invention. The present invention also provides methods for eliciting an immune response to a tumor cell in an individual.
EP1704855A2 2-Cyclopenten-1-one and its Derivatives as Inhibitors of the NF-kappa B Factor 2-Cyclopenten-1-one and its derivatives comprising the cyclopentenone nucleus as inhibitors of the NF-κB factor, with anti-inflammatory, anti-proliferative, immunosuppressive, cytoprotective and antiviral activity, the substituents being selected among the ones which do not affect the NF- κB inhibitory activity.
US6951640 Imaging tumors using organometallic porphyrin The present invention covers halogenated derivatives of boronated phorphyrins containing multiple carborane cages having the formula which selectively accumulate in neoplastic tissue within the irradiation volume and thus can be used in cancer therapies including, but not limited to, boron neutron-capture therapy and photodynamic therapy. The present invention also covers methods for using these halogenated derivatives of boronated porphyrins in tumor imaging and cancer treatment.
CN103735733A Compound preparation containing lutein ester and preparation method thereof The invention provides a compound preparation containing lutein ester, which is taken orally. The compound preparation comprises the following raw materials in parts by weight: 0.3-10.1 parts of lutein, 0-12.2 parts of lycopene, 0.1-18.7 parts of beta-carotene, 0-6.3 parts of vitamin B1, 0-7.2 parts of vitamin B2, 12.6-33.8 parts of vitamin C, 0-10.6 parts of vitamin E, 18.15-42.75 parts of zinc gluconate, 0-126.6 parts of wolfberry extract and 0-89.5 parts of cassia seed powder. The compound preparation containing lutein ester provided by the invention is scientific and reasonable in prescription composition and content collocation, innovative and feasible in process, and both capable of reducing the raw material cost, and greatly improving the bioavailability and biological safety for taking, generating synergistic interaction, significantly preventing and treating AMD disease and helping to alleviate visual fatigue, so that the market application prospect is wide.
WO2013094722A1 Cancer cell-inhibiting ceramics and method for producing cancer cell-inhibiting ceramics, method for treating bone neoplasm, and use of β tricalcium phosphate porous granules having grain size of 1 to 10 μm Provided is a cancer cell-inhibiting ceramics comprising β tricalcium phosphate porous granules having a grain size of 1 to 10 µm that effectively controls proliferation of cancer cells. The β tricalcium phosphate porous granules have the effect of inhibiting proliferation of cancer cells by being taken up by the cancer cells of the afflicted site. Proliferation of cancer cells can be more effectively controlled by using β tricalcium phosphate porous granules having a granule size of 1 to 10 µm.
CN101700225A Fat emulsion injection and production method thereof The invention relates to a fat emulsion injection and a manufacture method thereof. As the fat emulsion injection contains oleic acid, the fat emulsion injection can provide enough and stable emulsion particles when used as the auxiliary emulsifier so as to overcome the defects of oil floating, enlarged emulsion particles and the like of the emulsion. The method for manufacturing the fat emulsion injection adjusts the production technology in the production process by adding oleic acid in oil phase so as to improve the emulsifying capability, reduce the grain size of the emulsion particles, improve the stability of emulsion particles, reduce the value of methoxyaniline, reduce the number of homogenization, and improve the production yield.
EP2178852A1 Alkylsulfonyl-substituted thiazolide compounds A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus.
US20080318920 Deuterium-enriched ezetimibe The present application describes deuterium-enriched ezetimibe, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
EP1517667A2 Compositions and methods for reduction of inflammatory symptoms and/or biomarkers in female subjects Medicaments and methods for the treatment and/or amelioration of certain inflammatory symptoms related to premenstrual syndrome (PMS), premenstrual dysphoric disorder (PMDD), perimenopause, menopause, endometriosis, post-partum depression, or administration of hormonal contraceptives are described herein. Medicaments of the invention comprise a tocopherol, an omega-3 poly-unsaturated fatty acid, such as docosahexaenoic acid (DHA), or omega-9 polyunsaturated fatty acid, optionally, a flavonoid, and, optionally, a mineral, such as magnesium. Methods for treating or ameliorating such symptoms and methods for reducing elevated CRP and/or white blood cell (WBC) associated with such conditions using medicaments of the invention are also described.
WO2013139796A1 Use of amphoteric surfactants for the prevention and treatment of pathogenic vaginal biofilms in vaginal infections The invention relates to amphotheric surfactants for use in preventing and/or treating vaginal infections, in particular for preventing and treating pathogenic vaginal biofilms in vaginal infections, as well as to pharmaceutical compositions containing the amphoteric surfactants as active ingredients.
CN102746255A Compound having anti-tumor activity, and preparation method and application thereof The invention relates to the field of medicinal chemistry, in particular to a compound (I) having anti-tumor activity, a preparation method and an application of the compound (1), and a medicinal composition containing the compound (1), wherein the definitions of R and X are shown in the specifications. As proved by pharmacological testing, the compound provided by the invention has superior anti-tumor activity.
CN101301286B Applicaion of brasilein for preparing medicine for treating diseases caused by excess malondialdehyde generated in brain tissue in oxygen-glucose deprivation state The invention discloses novel use for brasilein, which relates to the novel use of the brasilein with brazilwood as raw material in the medical aspect, in particular to an application of the brasilein in the preparation of medicines used to treat cerebral ischemia or cerebral hemorrhage, brain tissue peroxide increase and brain function damage diseases caused by the brain tissue peroxide increase. As shown in experimental research, the brasilein has the effects on resisting oxidation, protecting brain neurons, enhancing cerebral blood flow, and suppressing the activity of erythrocyte membraneNa-K-ATP enzyme. The brasilein has an apparent effect on brain issue damage caused by cerebral ischemia reperfusion. When the diseases are treated, the brasilein, taken as an active ingredient, is independently used or matched with other medicines to prepare various medicines with different preparation formulations, and the medicines can be clinically used.
WO2009103932A1 Use of a cardiac glycoside and/or a diuretic for the treatment of neuropathic pain The invention comprises pharmaceutical compositions for the treatment of neuropathic pain, e.g. that associated with neuralgia, dystrophy or phantom limb pain. The pharmaceutical composition comprises cardiac glycosides and/or diuretics and is preferably topically applied in e.g. a gel. The invention also comprises methods of manufacturing such compositions.
US20120232087 Methods and compositions for treating solid tumors and other malignancies A combination of a kinase inhibitors of mTOR and downstream effector and a hedgehog pathway inhibitor for the treatment of cancer.
EP1824854A2 Substituted pteridines for treating inflammatory diseases The invention relates to novel pteridines which are suitable for treating respiratory or gastrointestinal complaints or diseases, joint, skin or eye inflammatory diseases, disease of the periphery or central nervous system or cancer. The invention also relates to pharmaceutical compositions containing said compounds.
CN1927273A Bath agent for influenza defervesce and preparing method thereof The invention provides a defervesce lotion for treating common cold and its preparing process, wherein the medicinal raw materials include root of Dahurain angelica 6-9 weight parts, ledebouriella root 8-12 weight parts, bupleurum root 12-18 weight parts, kudzuvine root 12-18 weight parts, plaster stone 20-30 weight parts, honeysuckle 20-30 weight parts, isatic root 12-18 weight parts, licorice root 4-6 weight parts and capsule of weeping forsythia 10-35 weight parts.
CN103610907A Pharmaceutical composition for treating dental ulcer and preparation method thereof The invention discloses a pharmaceutical composition for treating dental ulcer and a preparation method thereof. The pharmaceutical composition is prepared from the following medicines in parts by weight: 10-20 parts of allicin, 20-40 parts of root of rehmannia, 20-40 parts of radix ophiopogonis, 10-40 parts of wolfberry fruit, 40-80 parts of liquorice, 30-50 parts of mint, 10-50 parts of flavoring agent and 1000-1600 parts of ointment base. The pharmaceutical composition is good in treatment effect, convenient to use and carry and small in toxic and side effects.
US7230017 For therapy of neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.
WO2009068989A1 Benzomorphan compounds The invention relates to Benzomorphan Compounds of Formula (I): wherein X, R1, R2, R3, R4, and R5 are as defined herein. These compounds are useful for treating constipation preferably constipation caused by mu-opioid agonist therapy.
WO2010090716A1 Heteroaryls and their use as pi3k inhibitors This invention provides compounds of formula (IA) or (IB): wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
CN1813857A Method for preparing particle, capsule and tablet of several miccron powders for reducing blood sugar and anti-fatigue The present invention relates to a health-care food with the functions of raising immunity, reducing blood sugar, resisting fatigue and prolonging life. Said health-care food can be made into granule preparation, capsule preparation and tablet preparation, and is made up by using micrometer codonopsis root powder, micrometer American ginseng powder, micrometer rhodiola root powder, micrometer tortoise plastron powder, micrometer turtle shell powder, micrometer methyl pyridine acid chrome powder and propolis powder and isomaltose alcohol powder through a certain preparation process.
US20100222315 Patient populations and treatment methods The invention provides 17α-ethynylandrost-5-ene-3β, 7β, 17β-triol for use in methods to treat, e.g., hyperglycemia or diabetes patients having a body mass index of at least about 31 (≧30.5, ≧31 or ≧32), wherein the patients are not concurrently treated with metformin and optionally another antidiabetic agent. In these methods, the patient will generally have a fasting insulin level of at least 4 μU/mL or another characteristic as described herein.
US20080220095 Red blood cells loaded with s-nitrosothiol and uses therefor Red blood cells can be loaded with low molecular weight nitrosylating agents, such as S-nitrosothiols, to act as a delivery system for NO+ groups to tissues. Loaded red blood cells can be used in methods of therapy for conditions which are characterized by abnormal O2 metabolism of tissues, oxygen-related toxicity, abnormal vascular tone, abnormal red blood cell adhesion, or abnormal O2 delivery by red blood cells. Such treatment of red blood cells can be extended to in vivo therapies, with the object to achieve an increase in the ratio of red blood cell S-nitrosothiol to hemoglobin.
WO2013054756A1 Treatment agent and/or prophylactic agent for side effects of cancer drugs [Problem] To provide a prophylactic agent and/or a treatment agent for side effects of cancer drugs. [Solution] This invention provides a prophylactic agent and/or a treatment agent for side effects of cancer drugs which contains ALA substances.
CN102336840A Triple-helical Tremellan, preparation method and application thereof The invention discloses triple-helical Tremellan, a preparation method and application thereof. The preparation method comprises the following steps of: extracting Tremellan components through water extraction and alcohol precipitation, removing protein by using an enzyme-Sevage combined method, performing dialysis, and purifying by using anionexchange chromatography and gel filtration chromatography, and performing vacuum freeze drying, separation and purification on the components to obtain the Tremellan. By the method for preparing the Tremellan, the natural structure and activity of the Tremellan are not influenced; and the method has low requirement on equipment and low cost, and is suitable for large-scale promotion, development and use in industrial production. The purified Tremellan is subjected to component analysis, structure identification and antioxidant activity research, and results show that the Tremellan has high activity of removing hydroxyl radicals and is a potential antioxidant substance.
CN102391356A Steroid n-glycoside analogue taking dihydro-pyranoid ring as D ring and preparation and application thereof The invention belongs to the technical field of organic chemistry, relates to an n-glycoside analogue and in particular relates to a steroid n-glycoside analogue taking a dihydro-pyranoid ring as a D ring and a preparation and an application thereof. The steroid n-glycoside analogue taking the dihydro-pyranoid ring as the D ring has significant inhibition effects against a variety of tumor cell strains, such as the cell strains of prostatic cancer, human neuroblastoma and the like, and can be used for preparing anti-tumor medicaments. The steroid n-glycoside analogue taking the dihydro-pyranoid ring as the D ring is prepared trough five-step reactions, namely oxidation, hydroxyl protection, reduction, selective oxidation and glycosidation, the preparation method is simple and the conditions are mild.
US20120189612 Compositions and methods for treating cancer while preventing or reducing cardiotoxicity and/or cardiomyopathy The present invention provides methods for treating cardiotoxicity, cardiomyopathy, and/or cancer in a subject, as well as related compositions and kits, that employ a therapeutic agent, or a nucleic acid sequence encoding a therapeutic agent, selected from apolipoprotein A-1 (ApoA1), an ApoA1 mimetic, an agent that increases expression of ApoA1, or a binding agent specific for oxidized ApoA1, where the therapeutic agent is effective in preventing or reducing the level of cardiotoxicity and/or cardiomyopathy induced by the chemotherapeutic.
WO2011140676A1 Rhizoma gastrodiae plant extract used to prevent and treat alzheimer disease and vascular dementia and mixed type diseases thereof and preparative method thereof The present invention discloses use of Rhizoma Gastrodiae plant extract containing parishin derivative in manufacture of medicaments for preventing and treating Alzheimer disease (AD), vascular dementia (VaD) and mixed type diseases thereof. The present invention also discloses the method for extracting and refining plant extract from Rhizoma Gastrodiae (Gastrodia elata Blume), wherein the effective constituent is parishin derivative, especially parishin A, B, C. The plant extract which is extracted by water or alcohol-water and refined and purified by chromatography contains parishin derivative whose content is more than 35%, especially more than 50%. The dosage forms of the present invention preferably include injection, tablets, capsules, soft capsules, oral liquid or drop pills etc.
CN103739653A Novel 23-oleanolic acid compound as well as preparation method and application of compound in preparation of glycosidase inhibitor medicine The invention discloses a compound 2-hydroxyl-3-carbonyl-23-oleanolic acid-1,4,12-triene-28-acid as well as a preparation method and application of the compound preparation of a glycosidase inhibitor medicine. An alpha-glucosidase inhibitor with high efficiency is extracted and separated from an akebia plant, a plant material is rich in source, an extraction preparation method is easy to operate, the plant can be used for a long time without being damaged when extraction is performed by adopting a plant fruit, and thus the economic benefit can be increased, and the environment friendliness is achieved; the monomeric compound is stable and easy to store. Pharmacological experiments prove that the inhibitory activity of the compound 2-hydroxyl-3-carbonyl-23-oleanolic acid-1,4,12-triene-28-acid is stronger than that of a first-grade diabetes drug acarbose by about 16 times, and thus the compound 2-hydroxyl-3-carbonyl-23-oleanolic acid-1,4,12-triene-28-acid can be expected to be further developed into a medicine for clinically treating type 2 diabetes mellitus and is good in prospect.
WO2008006561A1 Substituted isoxalines, pharmaceutical compositions containing same, methods of preparing same, and uses of same The invention relates to substituted isoxazolines according to the general formula (I) : in which A, R1, R2, R3, R4, Z, X, m, n, and p, are given in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted isoxazolines, to methods of preparing said substituted isoxazolines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases known to be at least in part mediated by HDAC activity or whose symptoms are known to be alleviated by HDAC inhibitors.
EP2257283B1 L-citrulline for treating erectile dysfunction L-citrulline for treatment of endothelial dysfunction and in particular of erectile dysfunction and a pharmaceutical composition comprising L-citrulline in combination with one or more substances selected from the group consisting of pycnogenol, aqueous extract of Viscum album, NADPH, tetrahydrobiopterin, folic acid and mixtures thereof.
WO2014049841A1 Therapeutic or preventive agent for meibomian gland dysfunction or meibomian gland blockage The objective of the present invention is to provide a new medicinal use of clarithromycin. The present invention is a therapeutic agent or a preventive agent for meibomian gland dysfunction or meibomian gland blockage and comprises clarithromycin as an active ingredient. The dosage form is preferably an eye drop or eye ointment.
US20120149669 22-Haloacetoxy-Homopregnacalciferol Analogs and Their Uses This invention discloses 22-haloacetoxy-homopregnacalciferol analogs and specifically 22-bromoacetoxy-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits relatively little calcemic activity and does not promote cellular differentiation off HL-60 leukemia cells, but rather kills the cells. This cell death activity is found in small cell lung carcinoma also, but not in prostate cancer cells. This compound thus causes specific cell death in the absence of changes in calcium levels and without general toxicity in an animal. Therefore it might serve as a useful therapy for treatment of some forms of cancer, such as leukemia and lung cancer.
EP2361623A1 Composition comprising a polyphenol salt and corresponding use Composition comprising a polyphenol salt, with a molecular weight of between 500 and 9000, and gelatine. The salt has pharmacological properties such as protecting the mucous in the digestive tract, as an astringent and as an anti-diarrhoea product. It is suitable for treating infant dysenteriform enterocollitis and exasperated intestinal flora. It is suitable for use both in adults and children and weening infants. Moreover, the polyphenolic component adsorbs the albuminoidal and mucilaginous substances, thereby preventing their harmful action from irritating the intestinal mucous and, also, the gelatine mechanically protects the inflammed mucous against acids and alkalines, The gelatine makes it possible to reduce the stomach irritation that could be caused by the polyphenol in patients who are sensitive to it. Thanks to the proline content in the gelatine, the systemic absorption of the polyphenol is inhibited.
US6869941 Combination of drospirenone and an estrogen sulphamate for HRT A pharmaceutical dosage unit comprising drospirenone and an estrogen sulphamate, such as an estradiol sulphamate or an estriol sulphamate for use in hormone replacement therapy is disclosed. This, combination therapy may comprise continuous or discontinuous administration of drospirenone and/or the estrogen sulphamate, such as weekly administration of both agents or weekly administration of the estrogen sulphamate and daily administration of the drospirenone.
CN103156700A Vagina embolism of regulating yak reproduction and preparation method thereof Provided is a vagina embolism of regulating yak reproduction. The vagina embolism of regulating yak reproduction is in a Y shape and is composed of a plastic skeleton, silicon rubber medicine slow release caps and a plastic digging rope. Two cylinder slice layer shape silicon rubber medicine slow release caps are sleeved on two upper forks of the Y-shaped plastic skeleton, and medicine release function is possessed. The silicon rubber medicine slow release caps are prepared by mixing silicon rubber, silicon rubber cross-linking agent, melatonin powder and stearic acid slow-release formulation according to a ratio and through injection molding. The vagina embolism of regulating yak reproduction plays a regulating role in a reproduction system and a endocrine system through the melatonin, changes yak estrus cycle, produces yak estrus, improves sleeping, increase weight of the yak and strengthens immunity and anti-ageing ability.
CN103304680A Beta-glucan, and extraction method and application thereof The invention relates to beta-glucan and an extraction method and application thereof. Specifically speaking, the invention discloses beta-glucan extracted from sporophore of Grifola frondosa and represented by a formula described in the specification; beta-glucan exerts an antineoplastic effect by activating an immune system and is expected to be developed into a novel antineoplastic drug.
EP2361242A1 Oxidase inhibitors and their use The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.
WO2009152431A1 P2y1 receptor antagonists The invention provides P2Y1 receptor antagonists of Formula (I); wherein R1-R3 are as defined in the specification, pharmaceutical compositions comprising the same, and the use of such antagonists in the treatment of a disease or condition that can be ameliorated by antagonizing a P2Y1 receptor, for example, platelet aggregation, atherosclerosis or thrombosis. The invention also provides conjugates comprising a P2Y1 antagonist that is covalently linked to a conjugant such as a dendrimer.
WO2012082718A2 3-methanesulfonylpropionitrile for treating inflammation and pain The present invention relates to purified 3-methanesulfonylpropionitrile or a pharmaceutically acceptable salt thereof, and a method for preparing such compound. The compound has at least 90% (w/w) purity. The present invention is also directed to a pharmaceutical composition comprises the purified compound and a pharmaceutically acceptable carrier. The present invention is further directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering 3-methanesulfonylpropionitrile or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.
WO2013115916A1 Combination therapy comprising gs-7340 and cobicistat for use in the treatment of viral infections The use of {9-[(R)-2-[[(S)-[[(S)-l-(isopropoxycarbonyl)ethyl] amino]phenoxyphosphinyl] -methoxy]propyl] adenine } and the hemifumarate form (tenofovir alafenamide hemifumarate) in combination with cobicistat is disclosed. In addition, the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and elvitegravir is disclosed.
CN103058937A Pyrimidine derivative and medicinal application thereof The invention relates to 4-(4-(3-(2-amino-4-hydroxy-6-methyl-5-pyrimidinyl) propyl) amino) phenyl)-1-chloro-3-butene-2-ketone and fumarate of a derivative thereof or a solvate thereof acceptable in pharmacology and an application thereof for preparing a medicine for treating and/or relieving and/or preventing influenza.
WO2011107007A1 Polyethylene glycol electrolyte granues and its preparing process A polyethylene glycol electrolyte granular preparation and its preparing process are provided. The polyethylene glycol electrolyte granular preparation comprises polyethylene glycol with the average molecular weight of 3000 to 4000 and electrolyte. The granule diameter of the polyethylene glycol electrolyte granule is 180 to 850μm.
US20080227695 reduced expression and/or function of Dlg (discs large) is an important factor for tumor formation; measuring the expression and/or function of Dlg Tumor formation and reduced transcription of both sFRP1 gene and sFRP2 gene were found in Dlg gene knock-out mice, and thereby the following has been provided: an agent for enhancing the expression and/or function of sFRP, containing a compound having an effect of enhancing the expression and/or function of Dlg; an agent for inhibiting tumor formation or an agent for preventing and/or treating a tumor disease, containing the agent for enhancing the expression and/or function of sFRP; a method of enhancing the expression and/or function of sFRP, comprising enhancing the expression and/or function of Dlg; a method of inhibiting tumor formation or a method of preventing and/or treating a tumor disease, comprising using the aforementioned enhancing agent or the aforementioned enhancing method; a non-human mammal that is deficient in one or both of Dlg alleles; a cell originating in the mammal; a method of identifying a compound, comprising using the mammal or the cell; and a method of examining a tumor tissue or a tumor cell, comprising measuring the expression and/or function of Dlg.
US7034018 Substituted pyrrole mannich bases to combat pain and allergic reactions The invention relates to substituted pyrrole Mannich bases of general formula (I), wherein R1=H, a C1-10-alkyl-, aryl, a heteroaryl- or an aryl, heteroaryl-, CN, Br—, Cl or OH radical bound by a C1-6 alkylene group, R2=CH(R4)N(R5)(R6), R3, R3′, R3″ identically or individually represent H, F, Cl, Br, CF3, CN, NO2, SO2NH2, NHR7, SR8, OR9, CO(OR10), CH2CO(OR11), COR15, a C1-10-alkyl-, aryl-, heteroaryl-aryl radical or a heteroalkyl radical bound by a C1-6 alkylene group, R4=an unsubstituted phenyl radical or a phenyl radical substituted at least with C1-4 alkyl, C1-3-alkoxy-, halogen-, a method for the production of the above-mentioned compounds, medicaments containing said compounds, and the use of said compounds in the production of medicaments. Said active ingredients are particularly suitable for pain therapy, and for treating inflammatory and allergic reactions, drug or alcohol abuse, diarrhoea, gastritis, ulcers, cardiovascular diseases, urinary incontinence, depressions, states of shock, migranes, narcolepsy, overweight, asthma, glaucoma, hyperkinetic syndrome, lack of drive, bulimia, anorexia, catalepsia, anxiolysis increasing vigilance and/or increasing libido.
CA2225022C New polymorphous form of doxazosine mesylate (form iii) A new crystalline and anhydrous form of doxazosin mesylate of Formula I (see formula I) is described. The new form is crystalline and anhydrous and is characterised in its X-ray spectrum by the following reflex positions of high and medium intensity: 8.49° 21.03° 11.72° 22.87° 16.03° 25.02° 18.29° Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and medicaments containing the new form of doxazosin mesylate are also described.
US20060229324 Quinazolin-4-one derivatives A medicament having an inhibitory activity against hematopoietic prostaglandin D2 synthase, which comprises as an active ingredient a compound represented by the following general formula (I) or a salt thereof: wherein X represents a group represented by the formula —N═C(R5)— or the formula —NH—CH(R5)—, R1, R2, R3, and R4 represent a hydrogen atom, a halogen atom, a C1 to C6 alkyl group, or a hydroxy group, R5 represents a C1 to C6 alkyl group or a C6 to C10 aryl group, and R represents an amino group.
WO2010018280A1 Use of p2x7 receptor antagonists to promote axonal growth and ramification The present invention relates to the use of P2X7 receptor antagonists capable of crossing the hematoencephalic barrier and pharmaceutically-acceptable vehicles, in addition to pharmaceutical compositions thereof, to produce medicaments intended for the treatment of illnesses or conditions associated with: a) absence of or reduction in axonal growth; b) axonal collateral loss; c) nervous lesion; d) loss or degeneration of synaptic connections. In addition, the use is described of said antagonists to promote axonal growth both in cultivated neurons and in transplanted neurons. A method is also included for producing neurons differentiated in vitro commencing from stem cells, comprising culturing said cells in the presence of a P2X7 antagonist, together with the culture obtained through the previously described method, and use thereof for production of medicaments intended for the previously detailed illnesses.
CN101987862A Sulfamoyl heteroaryl carboxylic ester derivative of glucocorticoids The invention discloses a sulfamoyl heteroaryl carboxylic ester derivative of glucocorticoids, a compound in formula (II), wherein X is unsubstituted or substituted heteroaryl or alkyl heteroaryl, and Drug is glucocorticoids drug in which carboxylic ester can be formed through OH groups, which can be optionally substituted.
EP1147214B1 A novel method for designing protein kinase inhibitors The present invention provides a method for identifying inhibitors of protein kinases. Methods are also provided for inhibiting protein kinase activity. Specific non-peptide protein tyrosine kinase inhibitor are provided. The protein kinases produced using the method of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, or immune system activity.
DE102004060041A1 Use of substituted cyclopropane acid derivative having dopamine receptor ligand activity to e.g. treat metabolic syndrome; reduce lipid in the plasma; lower free fatty acid in the plasma; and treat diabetic dyslipidemia Use of substituted cyclopropane acid derivative (I) or its salts for the manufacture of a medicine to treat metabolic syndrome. Use of substituted cyclopropane acid derivative of formula (I) or its salts for the manufacture of a medicine to treat metabolic syndrome. R1>1-20C alkyl, 2-20C alkenyl, 2-20C alkynyl, aryl, heterocyclyl (all optionally substituted with one more T1 or T2), or H; T1 : F, Cl, Br, I, CF3, NO2, N3, CN, COOH, COO(1-6C alkyl), CONH2, CONH (1-6C alkyl), CON(1-6C alkyl)2, cycloalkyl, 1-10C alkyl, 2-6C alkenyl, 2-6C alkynyl, O-(1-6C alkyl), O-CO-(1-6C alkyl), O-CO-(1-6C aryl) (sic), O-CO-(1-6C) heterocyclyl; PO3H2, P(O)(O-alkyl)2, 1-6C alkylene-P(O)(O-alkyl)2, O-P(O)(OH)2, O-P(O)(O-alkyl)2, SO3H, SO2-NH2, SO2NH(1-6C alkyl), SO2N(1-6C alkyl)2, S-(1-6C alkyl), S-(CH2)n-aryl, S-(CH2)n-heterocyclyl, SO-(1-6C alkyl), SO-(CH2)n-aryl, SO-(CH2)n-heterocyclyl, SO2-(1-6C alkyl), SO2-(CH2)n-aryl, SO2-(CH2)n-heterocyclyl, SO2-NH(CH2)n-aryl, SO2-NH(CH2)n-heterocycl yl, SO2-N(1-6C alkyl)(CH2)n-aryl, SO2-N(1-6C alkyl)(CH2)n-heterocyclyl, SO2-N((CH2)n-aryl)2 or SO2-N((CH2)n-(heterocyclyl)2, (where aryl or hetercyclyl is optionally substituted with 1-2 substituents chosen from F, Cl, Br, OH, CF3, SF5, NO2, CN, OCF3, O-(1-6C alkyl), 1-6C alkyl and NH2); T2 : C(NH)(NH2), NH2, NH-(1-6C alkyl), N(1-6C alkyl)2, NH(1-7C acyl), NH-CO-(1-6C alkyl), NH-COO-(1-6C alkyl), NH-CO-aryl, NH-CO-heterocyclyl, NH-COO-aryl, NHCOO-heterocyclyl, NH-CO-NH-(1-6C alkyl), NH-CO-NH-aryl, NH-CO-NH-heterocyclyl, N[(1-6C alkyl)]-CO-(1-6C alkyl), N(1-6C alkyl)-COO-(1-6C alkyl), N[(1-6C alkyl)]-CO-aryl, N[(1-6C alkyl)]-CO-heterocyclyl, N[(1-6C alkyl)]-COO-aryl, N[(1-6C alkyl)]-COO-heterocyclyl, N[(1-6C alkyl)]-CO-NH-(1-6C alkyl), N[(1-6C alkyl)]-CO-NH-aryl, N[(1-6C alkyl)]-CO-NH-heterocyclyl, N[(1-6C alkyl]-CO-N((1-6C alkyl)2, N[(1-6C alkyl)]-CO-N(1-6C alkyl)-aryl, N[(1-6C alkyl)]-CO-N(1-6C alkyl)-heterocyclyl, N(1-6C alkyl)-CO-N(aryl)2, N(1-6C alkyl)-CO-N(heterocyclyl)2, N(aryl)-CO-(1-6C alkyl), N(heterocyclyl)-CO-(1-6C alkyl), N(aryl)-COO-(1-6C alkyl), N(heterocyclyl)-COO-(1-6C alkyl), N(aryl)-CO-aryl, N(heterocyclyl)-CO-aryl, N(aryl)-COO-aryl, N(heterocyclyl)-COO-aryl, N(aryl)-CO-NH-(1-6C alkyl), N(heterocyclyl)-CO-NH-(1-6C alkyl), N(aryl)-CO-NH-aryl, N(heterocyclyl)-CO-NH-aryl, N(aryl)-CO-N(1-6C alkyl)2, N(heterocyclyl)-CO-N(1-6C alkyl)2, N(aryl)-CO-N(1-6C alkyl)-aryl, N(heterocyclyl)-CO-N(1-6C alkyl]-aryl, N(aryl)-CO-N(aryl)2, N(heterocyclyl)-CON(aryl)2, aryl, O-(CH2)n-aryl or O-(CH2)n-heterocyclyl (where the aryl- or heterocyclyl- residue is substituted with 1-3 substituents of F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O-(1-6C alkyl), 1-6C alkyl, NH2, NH(1-6C alkyl), N(1-6C alkyl)2, SF5, SO2-CH3, COOH, COO-(1-6C alkyl) or CONH2); R2>1-20C alkyl, 2-20C alkenyl, 2-20C alkynyl, aryl, 3-7C cycloalkyl, heterocyclyl (all substituted with T1 or T2); R3>-R6>H, F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, 1-6C alkyl or O-(1-6C alkyl); and n : 0-6. [Image] - ACTIVITY : Antidiabetic; Antilipemic; Vasotropic; Antiarteriosclerotic; Cardiant; Cerebroprotective; Anticoagulant; Thrombolytic; Hypotensive; Cardiovascular-Gen.; Analgesic; Antianginal. The ability of (I) lower free fatty acid, glycerol or triglyceride in the plasma was tested using biological assays. The results showed that 1R-methoxycarbonyl-2R-hydroxycarbonylcyclopropane exhibited a median effective concentration value of 0.07 mu M. - MECHANISM OF ACTION : Dopamine receptor ligand.
US20140045885 Decoquinate, 4-hydroxyquinolones and napthoquinones combined with levamisole, Imidazothiazole, for the prevention and treatment of sarcocystosis and equine protozoal myeloencephalitis caused by Sarcocystis and Neospora and other apicomplexan protozoans. Apicomplexan parasites that infect horses such as Sarcocystis sp., Sarcocystis neurona and Neospora hughesi may be killed with decoquinate, a 4-hydroxyquinolone and/or a naphthoquinone and enhanced effects for treatment of animal disease are seen with the addition of levamisole, imidazothiazole. Based on such parasite-killing activity, these compounds are used in methods of preventing and treating infections, neurological disease or dysfunction such as protozoal myeloencephalitis, especially equine protozoal myeloencephalitis.
CN1846671A Oral solution containing alfacalcidol The present invention relates to medicine technology, and is especially one kind of oral solution containing alfacalcidol. The oral solution contains: alfacalcidol in therapeutically effective amount, therapeutically acceptable organic acid supplementary material in such amount as to regulate the pH value of the or al solution to 2.0-4.0, and water. The oral solution containing alfacalcidol has high stability.
CN102716142A Application of icariin to preparation of medicine for treating parkinsonism The invention discloses application of icariin to preparation of a medicine for treating parkinsonism. Through research, the icariin can be used the medicine for treating parkinsonism, the efficacy of the icariin is proved through experiment, and the icariin has an obvious treatment effect on parkinsonism. According to the icariin, materials are wide in source and easy to acquire, and the medicine can be easily prepared from icariin, and is good in treatment effect.
US7863446 Heterocycles Novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof are described. These compounds are useful in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell-damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever. More particularly these compounds are useful as PDE4 inhibitors, and useful for treating PDE4 mediated diseases.
EP0937153B1 Human monoclonal antibodies specific for hepatitis c virus (hcv) e2 antigen The present invention relates to compositions derived from immunoglobulin molecules specific for the hepatitis C virus (HCV). More particularly, the invention is related to molecules which are capable of specifically binding with HCV E2 antigen. The molecules are useful in specific binding assays, affinity purification schemes and pharmaceutical compositions for the prevention and treatment of HCV infection in mammalian subjects. The invention thus relates to novel human monoclonal antibodies specific for HCV E2 antigen, fragments of such monoclonal antibodies, polypeptides having structure and function substantially homologous to antigen-binding sites obtained from such monoclonal antibodies, nucleic acid molecules encoding those polypeptides, and expression vectors comprising the nucleic acid molecules.
CA2224164C Intrauterine chemical necrosing method and composition A method and composition for effecting chemical necrosis of a tissue lining of a mammalian body cavity, particularly a uterine endometrium, by delivering a caustic tissue necrosing composition, e.g., a silver nitrate and dextran paste, to the tissue to be necrosed and allowing the paste to remain in contact with the target tissue for a period of time sufficient to chemically necrose substantially the entirety of the tissue lining, and then contacting the caustic composition with a deactivating agent, e.g., an aqueous sodium chloride solution, thereby rendering the caustic composition non-caustic, and then rinsing the cav-ity. Compositions and methods for delivering medicaments are also disclosed.
CA2711605A1 Neuroactive steroid compositions and methods of use therefor Provided are methods for ameliorating a symptom of a neuropsychiatric disorder in a subject. Also provided are methods for ameliorating at least one physical symptom or at least one psychological symptom resulting from tobacco cessation in a subject, methods for ameliorating a symptom of Alzheimer's disease or other cognitive disorder in a subject, methods for ameliorating a symptom of schizophrenia, schizoaffective disorder, or other psychotic disorder in a subject, methods for ameliorating a symptom of a depressive disorder in a subject, methods for ameliorating a symptom of bipolar disorder in a subject, methods for ameliorating a symptom of post-traumatic stress disorder or other anxiety disorder in a subject, methods for predicting a predisposition to suicide, suicidal ideation, suicidal behavior, or a combination thereof in a subject, methods for ameliorating a symptom of a pain disorder in a subject, methods for ameliorating a neurodegenerative disorder in a subject, methods for ameliorating a symptom of traumatic brain injury in a subject, methods for ameliorating a sleep disorder in a subject, and methods for improving cognitive functioning in a subject. In some embodiments, the methods include administering to a subject in need thereof an effective amount of a neuroactive steroid composition comprising pregnenolone (PG), allopregnanolone (ALLO), dehydroepiandrosterone (DHEA), pharmaceutically acceptable salts thereof, derivatives thereof, or combinations thereof.
US20120245130 Methods of Using Substituted Tetracycline Compounds to Modulate RNA A method for modulating RNA with tetracycline compounds is described.
US20080076761 Pharmaceutical compositions of clonazepam and method of use thereof The present invention includes benzodiazepine compositions formulated for intranasal administration, comprising a binary solvent system comprising a first solvent in which the benzodiazepine is soluble, the first solvent capable of penetrating nasal mucosal tissue, and a second solvent in which the benzodiazepine in less soluble. The compositions of the present invention may be used to treat a variety of disorders including, but not limited to, panic attacks, muscle spasms, anxiety, and seizures. In one aspect, the present invention relates to a fast-acting, clonazepam composition for transnasal administration that can be used for the treatment of seizure clusters.
WO2009146102A1 Methods for the treatment or prevention of diabetes mellitus and other metabolic imbalances The invention relates to methods for treatment and prevention of a metabolic imbalance, including diabetes mellitus and other related diseases or disorders, using an extract from a fruit of genus Elaeis.
CN103598622A Sea cucumber nutrient tablet and application method thereof The invention provides a sea cucumber tablet which comprises the following active components: peach seeds, myrrh, safflowers, bamboo shavings, tangerine peel, fructus evodiae, hypericum japonicum, poria cocos, loofah sponge, raw rehmannia roots, sargentodoxa vine, isatis roots, scutellaria, gypsum, sea cucumber, chitin, starch, dextrin, mannitol, sugar powder, and microcrystalline cellulose. The application method of the sea cucumber nutrient tablet comprises the following steps: A. chewing, that is, chewing 1-2 chewing tablets before meal every day for postoperative patients; B. infusion with water, that is, taking 1 chewing tablet infused with 50 ml of water after meal every day for postoperative patients. The sea cucumber nutrient tablet of the invention is simple in preparation, and reasonable in formula combination, can promote immune regulation, and increase wound healing speed.
CN103622940A Application of gossypol acetate in pharmacy The invention discloses a novel application of gossypol acetate in the field of pharmacy, and in particular relates to an application of gossypol acetate in preparing medicines for preventing, relieving and/or treating reye's syndrome, and belongs to the field of pharmacy. Reye's syndrome is a cryptogenic acute encephalopathy syndrome in the childhood phase, and studies discover that loss or mutation of MeCP2 gene has a direct causal relationship with the reye's syndrome, and loss of the MeCP2 gene can cause reye's syndrome developing on a mouse. Experiments indicate that the content of the MeCP2 gene in the brain of a rat can be remarkably increased by administrating the rat with gossypol acetate, so that the content of the MeCP2 gene in the brain of a patient can be remarkably increased by using the gossypol acetate for preventing, relieving and treating the reye's syndrome caused by MeCP2 mutation, the development of the nerve cell of the patient can be promoted, functions of the nervous system can be restored, and the possibility of healing the patient can be increased. Therefore, according to the application of the gossypol acetate in preparing the medicine for resisting reye's syndrome, the medicine can be used for preventing, relieving and/or treating the reye's syndrome.
CN1650855A Rabdosia rubescens injection agent and its preparation technology An injection of rebescensine A is prepared through dissolving rebescensine A in dimethyl sulfoxie, adding anhydrous sodium sulfate, dissolving, adding alcohol and dimethyl sulfoxide, coarse filtering, fine filtering, introducing N2 while sealing it in ampules, and sterilizing. Its advantages are high stability and high safety.
EP1676570A1 Topical pharmaceutical compositions comprising L-arginine and uses thereof The invention relates to a topical pharmaceutical composition such as a cream or an ointment for the improvement of the conditions of venous insufficiencies or skeletal muscles comprising as the active agent L-arginine or any pharmacologically acceptable L-arginine derivate together with conventional excipients and/or caffeine and/or vasoactive herbal ingredients and uses thereof. Animal experiments and a limited number of human trials indicate that L-arginine is rapidly absorbed through the skin and reaches the bloodstream within minutes, after which L-arginine (alone or in combination with other vasoactive compounds) affects blood vessels in cutaneous as well as in subcutaneous tissues. As disclosed, the benefits of applying L-arginine onto the skin (alone or in combination with other vasoactive agents) include: the improvements of (1) the conditions of venous insufficiencies (pains, aching, inflammation, swelling, edema), (2) the conditions of skeletal muscles (muscle fatigue, spasms, cramps, pains) and (3) (in the case of long-term application) the appearance of the aging skin (reduced depth of wrinkles and increased softness of the skin).
US20100310638 Liposomes comprising duramycin and anti-viral agents Disclosed are surprising discoveries concerning the role of anionic phospholipids and aminophospholipids in tumor vasculature and in viral entry and spread, and compositions and methods for utilizing these findings in the treatment of cancer and viral infections. Also disclosed are advantageous antibody, immunoconjugate and duramycin-based compositions and combinations that bind and inhibit anionic phospholipids and aminophospholipids, for use in the safe and effective treatment of cancer, viral infections and related diseases.
US20100330200 Combination of a retinoid and a platinum anticancer agent A combination comprising an atypical retinoid compound, preferably E-4-(3-(1-adamantyl)-4-hydroxyphenyl)cinnamic acid and an anticancer drug of the platinum family, preferably cisuplatin, together with a pharmaceutical composition comprising it and a kit for its administration in unitary or in coordinated sequential form. The kit preferably comprises a first formulation of E-4-(3-(1-adamantyl)-4-hydroxyphenyl)cinnamic acid dissolved in a mixture of ethanol and cremophor, and susupended in a saline solution, and a second formulation of cisuplatin in saline solution. The combination is used for the preparation of a medicament to inhibit tumor growth and tumor migration, in particular for the treatment of ovarian tumor and/or carcinoma.
US20110293575 Photochemical internalisation of kinase inhibitors The present invention relates to a method for enhancing the activity of kinase inhibitors in target cells, and more specifically for enhancing the activity of tyrosine kinase inhibitors (TKIs), said method comprising contacting a cell with a kinase inhibitor and a photosensitizing agent and irradiating said cell with light of a wavelength effective to activate the photosensitizing agent, and to the use of this method for enhancing the effects of kinase inhibitors or kinase inhibitor-based drugs in particular to achieve cell death, for example, in cancer treatment and other diseases or conditions in which kinase inhibitors, such as TKIs, have a beneficial effect.
US20120027690 Ph-sensitive graft copolymer, manufacturing method for same, and polymer micelles using method The present document relates to a manufacturing method for pH-sensitive graft polymer micelles and a polymer micelle-type pharmaceutical composition containing the graft copolymer. The pH-sensitive graft copolymer micelles are usable as various markers and contrast agents for various molecular images for the diagnosis and treatment of diseases and a carrier for delivery of various medicines according to disease. The pH-sensitive graft copolymer forms micelles that can be used in target-oriented diagnosis and medicine release according to changes in the pH of a body. The polymer micelles are provided by inducing a graft copolymer of poly(β-amino ester) compounds which has a solubility in water depending on pH but is incapable of forming the micelles due to a self-assembly phenomenon, and hydrophilic poly(ethylene glycol) compounds.
US20130059815 Nutritional compositions containing human milk oligosaccharides and methods for using the same This disclosure features human milk permeates and compositions containing the same obtained from fractionated whole human milk. The oligosaccharide rich permeate and permeate compositions of the present invention are useful as nutritional supplements for pre-term and full term infants, for establishing or maintaining gut flora and for treating the symptoms of inflammatory bowel disease.
CA2577191A1 4-heteroarylmethyl substituted phthalazinone derivatives A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NRx or CRxRy; if X=NRx then n is 1 or 2 and if X=CRxRy then n is 1; Rx is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; Ry is selected from H, hydroxy, amino; or Rx and Ry may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or when X is CRxRy, RC1, RC2, Rx and Ry, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R1 is selected from H and halo; and Het is selected from: (i) formula (i), where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N, where only one or two of Y1, Y2 and Y3 can be N; and (ii) formula (ii), where Q is O or S.
WO2014022728A1 Substituted 5 - (quinazolin - 2 - yl) pyrimidin- 2 -amine derivatives useful as pi3k/mtor inhibitors for the treatment of cancer The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds of formula (I) and pharmaceutically acceptable salts, prodrugs, and solvates thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
US20120022136 Cellular Genes Regulated by HIV-1 Infection and Methods of Use Thereof This invention provides cellular gene products which have anti-apoptotic activity in HIV-1 infected cells and provides agents for the inhibition of the cellular gene products.
CN102670514A Agomelatine solid preparation The invention provides an agomelatine solid preparation. Agomelatine and a carrier are subjected to hot melt extrusion to form solid dispersoid of agomelatine, and the solid dispersoid of agomelatine can be further prepared into the solid preparation. A product can be dissolved out well and is controllable in quality.
US6858597 Halogenated sulphamate-, phosphonate-, thiophosphonate-, sulphonate- and sulphonamide- compounds as inhibitors of steroid sulphatase A compound is described. The compound has the formula (Ia) as presented in the FIG. 1; wherein: X is a ring having at least 4 atoms in the ring; K is hydrocarbyl group; Rh1 is an optional halo group; Rh2 is an optional halo group; at least one of Rh1 and Rh2 is present; Rs is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group. The compound is capable of inhibiting steroid sulphatase (STS) activity.
EP1816128A1 Carboxylic acid derivative containing thiazole ring and pharmaceutical use thereof According to the present invention, a compound represented by the following formula (I) having a superior PPARα, agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.
US20110130458 Krill oil process The present invention relates to a process for preparing compositions of high concentrations of omega-3 fatty acids from krill. Furthermore, the invention relates to a composition comprising high concentrations of omega-3 fatty acids, and a lipid fraction from krill comprising high amounts of fatty acids with chain length C14 and C16.
US20110123651 Dietary supplement drink for delivery of resveratrol and other polyphenols A nutritional beverage or drink is provided having resveratrol mixed with water, suspended in a liquid suspension system. One or more of quercetin, catechins, antioxidants, energy agents, sweeteners, preservatives, pH balancing ingredients, and coloring agents may also be included. A process is provided for preparing a dietary supplement drink in a liquid suspension, comprising mixing water in a suspension system with resveratrol. The process may also include adding one or more of quercetin, catechins, antioxidants, energy agents, sweeteners, preservatives, acidulants, and coloring agents. The nutritional beverage or drink may also be modified by using pure water that has nanosized water clusters therein, as well as mixing into the liquid suspension nanoparticles of resveratrol and/or one or more of the above ingredients to enhance the bioavailability of the ingredients. The compositions may be used to treat diseases and bodily malfunctions.
CN103520139A Inhaled quercetin nanometer-particles and preparation method thereof The invention relates to inhaled quercetin nanometer-particles. The inhaled quercetin nanometer-particles comprise 1-5 parts of quercetin, 1-20 parts of chitosan or derivative of the chitosan, 1-10 parts of phospholipid or a derivative of the phospholipid and 1-10 parts of excipient. The chitosan or the derivative of the chitosan is one or more of chitosan, chitosan oligosaccharide, quaternary ammonium salt of chitosan and carboxymethyl chitosan at high molecular weight, mediate molecular weight and low molecular weight. The diameter of each inhaled quercetin nanometer-particle ranges from 100 nanometers to 0.49 micrometer. The quercetin is prepared into a powder slow-release nanometer-particle inhalant and directly plays a role in the lungs, so that the defects that the quercetin is not soluble in water, absorption of the quercetin is difficult, and the quercetin is prone to oxidization are overcome, the bioavailability of the quercetin is improved, slow release can reduce a dosage, and the problems that a patient is poor in compliance, no specific treating medicine for radioactive damage is provided are solved by inhalation. The inhaled quercetin nanometer-particles have the power characteristics of the appropriate diameter, the appropriate form and like and has the slow release property. A preparation method of the quercetin nanometer-particles breathed into the lungs has the advantages of being easy and convenient to operate, stable in technology, capable of enabling industrial production to be easily achieved and the like.
EP1896010A2 Method and composition to treat skin ulcers The invention is directed to a method for treating ulcers, including ulcers of the lower leg, by topical plus oral administration of proanthocyanidins to a patient.
WO2010112092A1 Compounds for treatment of duchenne musculary dystrophy Compounds of formula (I) wherein R1, R2, R3, R4, L1, and n are as defined herein, are useful for the treatment or prophylaxis of conditions such as Duchenne muscular dystrophy, Becker muscular dystrophy, and cachexia.
EP1785484B1 Oligonucleotide inhibiting tumor cell proliferation and method therefor [PROBLEMS] It is found out that NEK2 kinase (accession number NM_002497) is expressed specifically in tumor cells such as bile duct cancer cells. It is further found out that the proliferation of such tumor cells can be inhibited by inhibiting the expression of the NEK2 kinase by the RNA interference method. [MEANS FOR SOLVING PROBLEMS] A tumor (for example, bile duct cancer) proliferation inhibitor which contains, as the active ingredient, an oligoribonucleotide corresponding to a base sequence of 30 or less consecutive bases in the base sequence of SEQ ID NO:1 which at least contains 19 consecutive bases in the base sequence of SEQ ID NO:1 (NEK2 gene) such as bases of nos. 403 to 423, 507 to 527 or 989 to 1009, an oligoribonucleotide complementary thereto, or a double-stranded RNA comprising the same.
WO2013050930A1 Development of a red clover phytoestrogen product for the prevention or treatment of osteoporosis Using computational modelling and entropic analysis (the Pharmaceutical Platform Technology), various pharmaceutical compositions derived from Red clover (Trifolium pratense) extracts comprising lsoflavones have been developed. Said compositions include an immediate release formulation comprising alpha-cyclodextrin, a sustained release formulation that comprises polyvinylpyrrolidone as an excipient, and a combined formulation comprising the aforementioned immediate release and sustained release compositions. The isoflavones of interest include biochanin A, formononetin, daidzein, equol, and genistein. The resulting pharmaceutical compositions are useful in the treatment and prevention of osteoporosis.
EP1544207A1 Process for producing glycoside A glycoside in which at least two phenolic hydroxyl groups of a compound having at least two phenolic hydroxyl groups in its molecule are glycosidically linked to anomeric carbon atoms of at least two sugar molecules can be prepared with high yield by a method including the step of allowing phenolic hydroxyl groups of a compound having at least two phenolic hydroxyl groups in its molecule to react with sugar molecules each having an acetylated hydroxyl group attached to an anomeric carbon atom in the presence of an organic solvent and an acid catalyst while removing acetic acid formed during the reaction from the reaction system.
US20080227851 psoriasis, eczema, multiple sclerosis, and arthritis; cross-metathesis reaction being promoted by a cross-metathesis catalyst Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.
US20120302610 Picolinamido-propanoic acid derivatives useful as glucagon receptor antagonists The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
CN101804198A Combination containing fotemustine The invention relates to a combination containing fotemustine, which comprises an antitumor active ingredient, a thymus preparation and auxiliary materials, wherein the antitumor active ingredient is the fotemustine, the thymus preparation is an immunopotentiator, and the auxiliary materials comprise disodium hydrogen phosphate, hydrochloric acid, poloxamer, sorbitol, tween 80, mannitol and benzyl alcohol. By organically combining the immunopotentiator and the fotemustine which has favorable curative effect but larger toxicity, the invention effectively improves the drug effect, and greatly lowers the drug toxicity meanwhile.
US20110129541 Suspension delivery system for the sustained and controlled local release of pharmaceuticals The invention relates to a novel suspension delivery system for the sustained and controlled release of pharmaceuticals. Methods of preparation and use are also disclosed.
EP2448945A1 Crystalline forms of prasugrel salts Salts of prasugrel were prepared including, for example, crystalline forms of prasugrel hydrobromide. These salts are useful, for example, in medicaments that inhibit the aggregation of platelets.
CN101020047A Health food containing calcium reinforcing agent The present invention discloses one kind of health food containing calcium reinforcing agent. The health food connects natto kinase or fermented soybean streptokinase in 100-5000 U/g and calcium reinforcing agent in 40-80 wt%. The health food of the present invention has the raised health effects of promoting calcium absorption with vitamin D3, promoting the chelating between bone and calcium with vitamin K2, lowering blood sugar, blood fat and blood pressure, preventing thrombus, etc. The present invention is suitable for all people, especially middle-aged people and old people.
US20100015080 Use of at least one (dihydro)jasmonic acid derivative for treating dry skin A cosmetic process for treating dry skin and/or a dry scalp of non-inflammatory origin, for example, in a menopausal woman, comprising topically applying to the skin and/or the scalp a composition comprising, in a physiologically acceptable medium, at least one (dihydro)jasmonic acid derivative; novel (dihydro)jasmonic acid derivatives and to the compositions, for example, suitable for topical application to the skin, comprising them.
US7144896 heterocyclic imines such as 3-[6-(1-Methanesulfonyl-1-methyl-ethyl)-quinolin-8-yl]-N-[6-(4-methylsulfanyl-phenyl)-pyridin-3-yl]-benzamide, used as phosphodiesterases (pde4) inhibitors; side effect reduction 8-arylquinolines wherein the aryl group at the 8-position contains a meta one or two atom bridge to a phenyl, 5 or 6 member heteroaryl or fused bicyclic heteroaryl group, and wherein at least one of the bridge atoms is not carbon, are PDE4 inhibitors.
CN101829045A Azithromycin slow-release dry suspension and preparation method thereof The invention provides an azithromycin slow-release dry suspension and a preparation method thereof. A sweet and aromatic azithromycin slow-release dry suspension is prepared by preparing bitter azithromycin into pellets, then wrapping with an isolation layer and a slow-release layer and mixing with auxiliary materials and the like. The invention adopts convention equipment and has creative preparation process, good taste, stable quality and good slow-release effect. Compared with common preparations, the azithromycin slow-release dry suspension has the characteristics of long onset time, sweet taste, particular suitability for children and excellent tolerance, therefore, a therapeutic schedule tends to be simple and convenient.
WO2014068296A1 Fat loss composition Disclosed is a fat loss composition comprising a) a prostaglandin F2alpha analogue, such as cloprostenol, or a pharmaceutically acceptable ester or salt thereof; and b) amino acids 176-191 of human growth hormone. Use of the composition in weight loss, weight management and/or slimming is described.
WO2010017355A2 Small molecule inhibitors of retroviral assembly and maturation Chemical compounds that disrupt retroviral assembly and maturation are presented herein. More particularly, this disclosure provides small molecule compounds that disrupt the formation and maturation of virus particles and methods of using such small molecules to treat HIV-1 infection.
CN103393614A Perospirone hydrochloride sustained release preparation and preparation method thereof The invention discloses a perospirone hydrochloride sustained release preparation for antischizophrenic therapy, which is characterized by tabletting with high-molecule hydrophilic gel skeletons; or preparing pellets through extrusion and rounding, coating with controlled release layers composed of water-insoluble polymers, and filling to prepare perospirone hydrochloride sustained release capsules; or preparing waxy pellets through melt extrusion and rounding, and filling to prepare sustained release capsules, wherein the weight of every 1000 prepared sustained release tablets is 180-220g, and the weight of every 1000 prepared sustained release capsules is 100-220g; by taking simulated gastric fluid as a medium, the release amounts of the perospirone hydrochloride sustained release tablets or capsules at 2 hours, 4 hours, 8 hours and 12 hours are respectively 10-30%, 30-50%, 50-75% and more than 75% of a labeled amount; and the pharmaceutical content in every tablet is 4-12mg/tablet.
US20120295969 Novel Muscle Relaxant Using Negatively Charged Gold with Choline In order to achieve muscle relaxing effect and anti-atrial fibrillation effect, the present invention provides gold nanoparticles complexes. Gold nanoparticles complexes include negatively charged gold nanoparticles bound to choline or spermidine through ionic bonds according to the purpose to be achieved, which form gold nanoparticles-choline complexes or gold nanoparticles-spermidine complexes. The complexes migrate to an acetylcholine receptor and then the ionic bonds of the complexes are broken, thereby inducing gold-sulfur bonds in the Cys loop of an acetylcholine receptor, thus block the ionic path and achieve the effects.
CN103446045A Stable busulfan injection The invention provides a busulfan injection which is simple in prescription and stable in quality. The injection is prepared by the followings method: (1), dissolving busulfan into a mixed solvent of N, N-dimethyl acetamide and polyethylene glycol 400 in a volume ratio of (17-57):(83-43) to obtain a busulfan solution with concentration of 1mg/mL-7.5mg/mL; and (2), filtering and filling in a sterile manner, wherein in the dissolving process of the step (1), the temperature of the solution is 4 DEG C-25 DEG C, or/and inert gases are charged in an operation process until the solution is saturated. Not only is stability of the busulfan injection obtained by the preparation method disclosed by the invention improved, but also the safety of the injection after long-time storage is effectively ensured. Meanwhile, other substances or other chemical components are not introduced in the preparation process, so that the medication safety is ensured, and the drug cost is also lowered.
US8796317 Use of 7-nitro-2,1,3-benzoxadiazole derivatives for anticancer therapy Derivatives of the heterocyclic compound known as 7-nitro-benzofurazan or 7-nitro-2,1,3-benzoxadiazole, are agents having a strong inhibiting activity towards members of the glutathione S-transferase (GST) superfamily that are hyperexpressed in cancer cells, and make them particularly resistant to many stress factors. These compounds are useful in the production of pharmaceutical drugs to be used in anticancer therapy, and may be employed either alone or in combination with other chemotherapeutic agents.
CN101011413B Use of hydrogen sulfide and its donor sodium hydrosulfide in the production of medicaments The invention relates to a method for using hydrogen sulfide and relative donator as sodium bisulfide in the drug preparation. The invention uses exogenous hydrogen sulfide and relative donator as sodium bisulfide, via serial animal models and external tests to prove that said hydrogen sulfide and relative donator as sodium bisulfide can be used to treat several cardiovascular diseases, or reducethe active oxygen, accelerate the vessel growth, negative inotropic action, or calcium antagonist. Said cardiovascular diseases comprise myocardial infarction, fibrosis, or the like.
CN101401789A Cordyceps sinensis polysaccharide liposome medicament and preparation thereof The invention relates to liposome of extract of cordyceps and a method for preparing the same. The main composition of the extract is polysaccharide. The liposome of the cordyceps is prepared by using phospholipid and cholesterol as membrane materials, and the prepared liposome of the cordyceps can be further prepared into dosage forms of tablet, injection, oral agent, capsule, granule, freeze-dried powder and the like. The method for preparing the liposome of the cordyceps can adopt a reverse evaporation method, a film ultrasound method and an ethanol injection method, the encapsulation rate of the methods can reach more than 40 percent, and the in vitro burst rate is low. The preparing process improves the stability of the drug. After the polysaccharide of the cordyceps is coated with the liposome, the polysaccharide of the cordyceps can be absorbed and used better in human body; and through the slow release effect of the liposome, the effective blood drug level of the drug can be maintained for a longer time.
US20110189306 COMPOUNDS, COMPOSITIONS AND TREATMENTS FOR V-ATPase RELATED DISEASES The present invention relates to therapeutic and/or prophylactic uses of hydrazide compounds and to pharmaceutical compositions containing one or more of these compounds as an active component for treating a disease or disorder requiring modulation of vacuolar (H+)-ATPases.
US20110223153 Modified silk films containing glycerol The present invention provides for compositions and methods for preparing aqueous insoluble, ductile, flexible silk fibroin films. The silk films comprise silk fibroin and about 10% to about 50% (w/w) glycerol, and are prepared by entirely aqueous processes. The ductile silk film may be further treated by extracting the glycerol from and re-drying the silk film. Active agents may be embedded in or deposited on the glycerol modified silk film for a variety of medical applications. The films may be into 3-dimentional structures, or placed on support surfaces as labels or coatings. The glycerol modified silk films of the present invention are useful in variety of applications such as tissue engineering, medical devices or implants, drug delivery, and edible pharmaceutical or food labels.
US7273867 Anticaogulants; cardiovascular disorders; Factor x inhibitors; antiinflammatory agents Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders
CN103275024A Azole antifungal compound and its preparation method and application The invention provides an azole antifungal compound and its pharmaceutically acceptable salt. The structural general formula of the azole antifungal compound is as shown in the specification, wherein R is selected from various aliphatic primary amine or secondary amine, aromatic primary amine or secondary amine and various substituted phenylpiperazine; the substituent group on phenyl of the substituted phenylpiperazine is hydrogen, alkyl group, halogen, cyanogroup, nitro-group, amino group or alkoxy group, is arranged at ortho, meta or para position of phenyl ring, and is monosubstituted or polysubstituted; the alkyl group is the alkyl group with 1-4 carbon atoms; the halogen is selected from F, Cl, Br or I; and the alkoxy group is selected from methoxy, ethoxy and t-butyl oxygroup. The compound provided by the invention has strong antifungal activity to deep fungi. In comparison with present antifungal drugs applied in clinic, the compound provided by the invention has advantages of high efficiency, low toxicity, wide antifungal spectrum and the like. Thus, the compound can be applied to prepare antifungal drugs. A preparation method of the compound is simple and has high yield. The prepared compound has a good antifungal effect.
CN102920828A External adhesive plaster for treating rheumatism and ostalgia and preparation method of external adhesive plaster The invention discloses an external adhesive plaster for treating rheumatism and ostalgia and a preparation method of the external adhesive plaster. The external adhesive plaster is prepared from toddalia asiatica, cudweed herb, climbing entada, polygonum cuspidatum, radix stephaniae tetrandrae as well as a proper amount of tea oil and red lead. The preparation method comprises the following steps of: firstly, respectively weighting all the raw materials for later use; placing all the raw materials into a container, and injecting the tea oil into the container; soaking the raw materials into the tea oil, sealing the opening of the container, after soaking for one day, pouring the drugs in the container into a pot to decoct until the drugs are carbonized, filtering residues to obtain a medical oil, heating the medical oil and cooking until oil drips form balls, and then, adding the red lead to stir to form a black thick paste liquid; and placing the obtained paste liquid into water to soak for 2-4 days to obtain the external adhesive plaster. The external adhesive plaster has the effects of dispelling wind and eliminating dampness as well as activating meridians to stop pain and has an obvious curative effect for various diseases caused by arthralgia syndromes.
WO2009080745A3 Perhydroquinoxaline derivatives as analgesics The present invention relates to perhydroquinoxaline derivatives, to a process for preparation thereof, to the use thereof for production of a medicament, and to medicaments comprising perhydroquinoxaline derivatives.
CN102125693A Tiagabine hydrochloride pharmaceutical composition and preparation method thereof The invention provides a tiagabine hydrochloride pharmaceutical composition and a preparation method thereof. A carrier of the pharmaceutical composition is vitamin E polyethylene glycol succinic acid ester or adopts the combination of the vitamin E polyethylene glycol succinic acid ester and other carriers; and the novel tiagabine hydrochloride composition is prepared by adopting a melting method, a solvent method or a solvent-melting method under the non-aqueous condition. The preparation method can improve the stability of the tiagabine hydrochloride pharmaceutical composition and simultaneously improve the extraneous dissolving rate of the pharmaceutical composition; the prepared pharmaceutical composition has higher dissolution and stability and is convenient for taking; and the pharmaceutical composition also has higher bioavailability and lower fluctuation performance.
WO2014051359A1 Pharmaceutical composition comprising neferine as active ingredient for preventing or treating hepatoma The present invention relates to a novel use of neferine for treating hepatoma, and more particularly, to a pharmaceutical composition and to a health functional food comprising neferine as an active ingredient for preventing or treating hepatoma. The neferine of the present invention can have an anticancer effect through the activities of stopping a cell cycle, inducing apoptosis and autophagy, and inhibiting angiogenesis and cell migration of hepatocarcinoma cells. In particular, since neferine has cytotoxicity specificity for hepatocarcinoma cells caused by viral infection even among hepatocarcinoma cells, the present invention has an effect optimized for treating hepatocarcinoma cells caused by viral infection. Thus, the neferine of the present invention can be used as a health functional food, as well as a medicine such as a pharmacological composition used as a material which can prevent or treat hepatoma. Therefore, it is expected that the value of the present invention is very high when the present invention is applied to the food industry and the pharmaceutical industry. Furthermore, since the neferine of the present invention does not show cytotoxicity for cells other than certain hepatocarcinoma cells, the composition of the present invention, which comprises neferine as an active ingredient, is beneficial in consideration of the safety of long-term use.
WO2013139918A1 Topical application of ingenol mebutate with occlusion The present invention relates to formulations of ingenol mebutate and methods of preparation and use thereof. More specifically, the invention relates to formulations of ingenol-3-mebutate applied to the skin with occlusion, and methods for treating or preventing diseases or conditions.
WO2006054119A1 Topical formulations for use in the treatment or prevention of dermatological conditions Topical compositions comprising a steroid selected from the group consisting of ethisterone and derivatives thereof and trilostane and derivatives thereof and the use of said steroids in the manufacture of a topical medicament for the prevention or treatment of a dermato logical condition that can be so prevented or treated by modifying the growth and interaction of one or more of blood vessels, adipocytes and fibroblasts and/or by modifying fibrosis.
WO2006097247A1 The use of non-steroidal anti-inflammatory drugs by inhalation in the treatment of acute and chronic bronchitis This invention claims the use of non-steroidal anti-inflammatory drugs, and in particular lysine acetylsalicylate, delivered by nebuliser, to treat non- asthmatic bronchitis, namely acute bronchitis, chronic bronchitis, emphysema and chronic obstructive pulmonary disease.
CA2620370A1 Extended release pharmaceutical composition of metformin and a process for producing it The present invention is directed to a pharmaceutical composition in the form of tablets, which constitute an orally administered, controlled drug delivery system that will provide increased retention time of the device in the stomach over conventional dosage forms and release metformin or its pharmaceutically acceptable salt in a controllable manner, and further that is easy and inexpensive to manufacture.
CN101112372A Application of compound s1 in the preparation of anti-cancer medicine The invention relates to the field of cell biology and provides the application of a compound s1 in the preparation of anti-cancer drugs. Cancer becomes a first cause of death, and the substances which can kill the tumor and the growth of the cancer cells also become the hot spot in research in the current biomedical field. The s1 of the invention can kill or inhibit a variety of tumor cells and cancer cells; at the same time, the compound s1 of the invention also has the inhibition effect of phosphate kinase Aurora-B. All these probe that the compound s1 of the invention has the inhibition effect of malignant tumors. The compound s1 of the invention can be linked with the suitable pharmaceutical acceptable carriers to prepare the anti-cancer drugs, so as to inhibit the continuous growth of the tumors.
CN103211799A Flurbiprofen paracetamol ester external use slow release transdermal patch and preparation method thereof The invention relates to a flurbiprofen paracetamol ester external use slow release transdermal patch and a preparation method thereof. The transdermal patch comprises a backing membrane layer, a drug-containing storage layer and an antistick layer, wherein, the drug-containing storage layer comprises 1-40 wt.% flurbiprofen paracetamol ester and 20-50 wt.% pressure-sensitive adhesive and 10-30 wt.% penetration promoter, as well as 0-20 wt.% additive optionally. The invention provides flurbiprofen paracetamol ester external use slow release transdermal patch has good percutaneous permeability and slow releasing effect, and can maintain effective plasma concentration of the affected part for 24 hours, and performs long-acting anti inflammatory and analgesic effect of the partial part with suitable viscosity, extreme low skin excitant and without obvious toxic and side effect. The patch is especially suitable for treatment of bone arthritis, rheumatoid arthritis, ankylosing spondylitis and other inflammations as well as symptomatic treatment of sprain, muscle strain and other soft tissue aches and postoperative aches.
US6903129 D-proline prodrugs The invention relates to compounds of formulas wherein R1 and R2 are independently from each other lower alkoxy, lower alkenyloxy, benzyloxy, hydroxy, —OCH(CH3)OC(O)-lower alkyl or —OCH2C(O)N(R3)(R4), with the proviso that only one of R1 or R2 may be hydroxy; R3 and R4 are independently from each other and signify hydrogen, lower alkyl, lower alkenyl or cycloalkyl; or R1 and R2 form together with the carbon atom, to which they are attached the linking group X, wherein X is —O(CH2)nCH═CH(CH2)nO— or —O(CH2)mO—; n is 1, 2 or 3; and m is 4-8, or a pharmaceutically acceptable salt of said compound. Compounds of the present invention can be used for the treatment of diseases where Serum Amyloid P Component depletion has a beneficial effect, in particular in the treatment or prevention of central and systemic amyloidosis.
CN102188363A Transdermal medicament delivery system containing donepezil compound, preparation and preparation method The invention discloses a transdermal medicament delivery system containing a donepezil compound, a transdermal preparation and a preparation method. The transdermal medicament delivery system comprises the following components in percentage by weight: 0.1 to 50 percent of donepezil or acid radical salt thereof, 1 to 95 percent of skeleton polymer, 0.1 to 60 percent of transdermal penetration enhancer, 0 to 10 percent of cross linker, 0.5 to 60 percent of humectant, 0.02 to 10 percent of bacteriostatic agent, 0.02 to 30 percent of pH regulator and 0 to 90 percent of solvent. The system is used for treating light, medium and severe senile dementia, can maintain long-time stable medicament delivery of at least 3 days, has better performance, is convenient for medicament delivery, and can reduce the administration frequency and increase the compliance of patients; and meanwhile, the transdermal path avoids first-pass effect on gastrointestinal tracts and liver due to oral administration of medicaments, and the system has higher bioavailability and obvious advantages in medicinal application.
CN101321744A Benzimidazole derivatives as gyrase inhibitors The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
WO2008034735A2 4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]diazepine derivatives The invention relates to 4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and claims, which are γ-secretase inhibitors and which may be useful in the treatment of Alzheimer's disease.
US20080103170 Nicotinic Acetylcholine Receptor Ligands Acetylcholine receptor ligands of formula I wherein D, E and G are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing, and methods for using the same.
US7166293 Anticancer agents; antitumor agents; cardiovascular diosrders; antiinflammatory agents A method for treating an angiogenesis-related disorder. The method includes administrating to a subject in need thereof an effective amount of a compound of the formula: Each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH═NOR, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.
WO2011009534A3 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl derivatives, methods for the production thereof and the use thereof for treating diseases The invention relates to 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl derivatives of formula (I) exhibiting progesterone-antagonistic effects and to methods for the production thereof, to the use thereof for the treatment and/or prophylaxis of diseases and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases, in particular uterine fibroids (myomas, uterine leiomyomas), endometriosis, menorrhagia, meningiomas, hormone-dependent mammary carcinomas and menopause-associated troubles, or for fertility control and emergency contraception.
EP2781520A1 Three-ring pi3k and/or mtor inhibitor The present application relates to a compound as represented by general formula (I), a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, preparation method of the compounds, a pharmaceutical composition containing the compounds, uses thereof in the preparation of drugs for treating and/or preventing proliferative diseases, and a method using the compounds to treat and/or prevent proliferative diseases. R1, R2, R3, R4, R5, R6, X, A and B in the formula are as defined in the specification.
CN101372471B Novel use of alkyl isourea compound and analogues thereof The invention discloses the new use of alkyl isourea compound and analogue of the alkyl isourea compound. The new use is the application of the alkyl isourea compound and the analogue of the alkyl isourea compound or salt which can be accepted by the the alkyl isourea compound and the analogue on pharmacy in the preparation of medicine for inhibiting leukemia cell proliferation and the application in the preparation of medicine for controlling and/or treating leukemia. The experimental results of anticancer cell proliferation in vitro shows that the alkyl isourea compound has better inhibition effect for leukemia cell line HL-60 of human body; wherein, when the drug concentration of the alkyl isourea compound is 12.5muM, the suppression ratio for the HL-60 reaches 94.22%.
CA2191440C Treatment and prevention of helicobacter infection An antigenic preparation for use in the treatment or prevention of Helicobocter infection in a mammalian host, comprises the catalase enzyme of Helicobacter bacteria, particularly the catalase enzyme of H. pylori or H. felis, or an immunogenic fragment thereof.
US20090130233 Two part lotion The present invention provides a composition, substantially a lotion, containing a source of nitrite ions and water. The composition, substantially a lotion, is preferably provided in two distinct and separate formulations. One of these formulations may or may not contain a source of nitrite ions. The composition is easily washed off with soap and water and is useful in preventing or treating bacterial, viral, parasitic or fungal infections. Further, the invention provides methods for preventing or treating bacterial, viral, parasitic or fungal infections by applying a pharmaceutically effective amount of the composition topically to the skin. Still further, the invention provides a kit comprising the composition of according to the invention together with instructions for applying the composition topically.
CN101897710A Medicament composition containing HMG-CoA reductase inhibitor, aspirin and folic acid and application thereof The invention relates to a fat-lowering medicament composition with synergy and application thereof. The fat-lowering medicament composition comprises an HMG-CoA reductase inhibitor with medicinal content, aspirin, folic acid or calcium folinate or levocalcium folinate and a pharmaceutically acceptable carrier. The medicament composition has pharmacological synergetic treatment effect which is shown in lowering blood fat, preventing and curing atherosclerosis and reducing a cardiovascular and cerebrovascular event risk. The invention also provides the application of the medicament composition to preparing a medicament for lowering the blood fat, preventing and curing the atherosclerosis and reducing the cardiovascular and cerebrovascular event risk. By applying the invention, the medicament composition with specific application, which is provided for a patient, can improve the compliance of the patient, is convenient for the patient to take medicines, reduces the medical expense and has more favorable market prospect.
CN100998560A Frozen emulsion containing polyene paclitaxel and its preparing method A freeze-dried emulsion of polyene taxol with a certain target performance and low poison is prepared from polyene taxol, the oil for injection, emulsifier, stabilizer, isotonic regulator, pH regulator, freeze-drying protector, and the water for injection. Its preparing process is also disclosed.
US20080009490 pyrazino[1,2-c]pyrimidine derivatives; viricide; infection by HIV, AIDS; with other HIV/AIDS antivirals, immunomodulators, antibiotics or vaccines; 2-(4-Fluorobenzyl)-9-hydroxy-7-[(1R,2S)-2-phenylcyclopropyl]-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,6,8(7H)-trione Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula I: wherein a, b, Y, R1, R2, R3 and R4 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
WO2008116670A1 Novel 5-cyano-prostacyclin derivatives and their use as agents for the treatment of autoimmune diseases This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1 - R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating autoimmune diseases. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
EP1775283A1 3-aminobenamide compound and vanilloid receptor 1 (vr1) activity inhibitor The present invention relates to a novel 3-aminobenzamide compound represented by the following formula which effectively inhibits vanilloid receptor subtype 1 (VR1) activity (wherein, for example, R1 is a C1-6 alkyl group which may be substituted, R2 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group which may be substituted, R3 is a hydrogen atom or a C1-6 alkyl group, R4 is a C1-6 alkyl group, a C1-6 alkoxy group, or a halo C1-6 alkyl group, m is an integer of 1 to 5 and P is a carbon or hetero ring) or a pharmaceutically acceptable salt thereof. The pharmaceutical composition comprising as active ingredients the 3-aminobenzamide compound or a pharmaceutically acceptable salt thereof is useful for treating diseases involved in VR1 activity such aspain, acutepain, chronicpain, neuropathic pain, rheumatoid arthritis pain, and neuralgia.
US20100240631 Pharmaceutical composition for the sublingual administration of progesterone, and method for its preparation A pharmaceutical composition is described for the sublingual administration of progesterone in the form of a rapidly-disintegrating tablet, which is capable of promoting a greater bioavailability of the progesterone; a method for preparing said pharmaceutical composition is also described.
CA2335065C Pharmaceutical formulations for aerosols with two or more active substances The present invention relates to new pharmaceutical formulations for aerosols with at least two or more active substances for administration by inhalation or by nasal route. Specifically, the invention relates to pharmaceutical preparations for propellant-driven metered dose aerosols using a fluorohydrocarbon (HFC) as propellant, which contain a combination of active substance of two or more active substances, wherein at least one active substance is present in dissolved form together with at least one other active substance in the form of suspended particles.
US7011093 Nasal dilators and strips, methods of their manufacture, and methods for improving the breathing of individuals are provided. The strips and dilators include an elongated substrate, with or without a dilating component or portion, Nasal dilators and strips, methods of their manufacture, and methods for improving the breathing of individuals are provided. The strips and dilators include an elongated substrate, with or without a dilating component or portion, having top and bottom surfaces and a pressure-sensitive adhesive disposed on the bottom surface. The dilator is designed to provide a gentle expanding force to the nasal wall tissue when the dilator is adhesively attached to the nose. This invention further includes a cosmetic fragrance, an aromatic medication and/or transdermal medication disposed on the strips or dilators. In order to improve the shelf-life and in-use olfactory effectiveness of such products, fragrance delivery mechanisms are used. Separation of volatile oils and adhesives are also provided to minimize adhesive residue.
CN101244060B Leonurus heterophyllus alkaloid composition The invention relates to a leonurus-japonicus alkaloid composition, belonging to the technical field of pharmacy; wherein, the proportion of the parts by weights of stachydrine and leonurine is 10 to 20:1; and both of stachydrine and leonurine have synergistic interaction and better pharmacologic effects.
CN101549145A Nutrient fluid capable of being radio-resistant and reducing side reaction of radiation treatment The invention discloses a nutrient fluid which is radio-resistant and reduces side reaction of radiation treatment. The nutrient fluid uses normal saline as the carrier of effective ingredients thereof and is most suitable for body gastrointestinal tract. All the effective ingredients in the nutrient fluid are dissolved and mixed in normal saline fully and absorbed by the human body effectively. The matching ratio of nutrient substances of the nutrient fluid is proper, especially by adding carotin, chitosan, vitamin C, vitamin E, radio-resistant and anti-oxidant functions of selenium and by supplementing deficient nutrient substances of glutamine and protein and the like, the repair function of intestinal tract function damage caused by radiation is promoted, not only full nutrition can be provided, the load of the intestinal tract is not increased, but also adjustment and repairing are carried out to flora and mucous membrane of different parts of gastrointestinal tract of the body, thus achieving the effects of improving body resistance and life quality. The nutrient fluid is prepared according to the characteristics of the patients, and has safe eating and no toxic side effect.
CN102240291A Imatinib-containing composition and preparation method thereof The invention relates to an imatinib-containing composition and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The imatinib-containing composition disclosed by the invention is composed of imatinib, a diluent, a disintegrating agent, an adhesive and a lubricant, wherein the imatinib is imatinib mesylate alpha crystal; the diluent is a mixture of microcrystalline cellulose and lactose; the disintegrating agent is cross-linked polyvidone; the adhesive is polyvidone K30; and the lubricant is a mixture of magnesium stearate, talc powder and silica micropowder. The preparation method is simple and efficient in process, and can be used for industrial mass production, and the problem that the imatinib mesylate alpha crystal has strong hydroscopicityis and is not easy to form preparation is completely solved.
CN102151300A Improved bromhidrosis powder The invention discloses improved bromhidrosis powder. The improved bromhidrosis powder consists of the following components in part by weight: 2 to 5 parts of yellow lead powder, 20 to 40 parts of clam meal, 2 to 6 parts of ground cloves, 6 to 20 parts of alum, 20 to 40 parts of talcum powder, and 20 to 40 parts of Jinmeng stone. The raw materials of the improved bromhidrosis powder are easy to obtain, and the preparation process is simple; the formula is scientific, the sterilization performance is high, and the deodorization effect is obvious and durable; and the improved bromhidrosis powder has no toxic and side effect on the human body and is not irritant to the skin, and is safe and convenient to use.
CN102584756A Novel monascuspurpurones, preparation process thereof, and uses of the monascuspurpurones The present invention relates to a novel monascuspurpurone compound of formula (I) as the description mentioned: or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR[gamma] and/or C/EBP[alpha], for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.
CA2754549A1 Enhancing coagulation or reducing fibrinolysis Methods for controlling bleeding (e.g., enhancing coagulation and reducing fibrinolysis) in a subject are disclosed. The methods include selecting a subject in need of enhanced coagulation or reduced fibrinolysis, and administering to the subject a carbon monoxide releasing molecule (CORM). Examples of CORMs include tricarbonyldichloro-ruthenium (II) dimer, tricarbonylchloro-(glycinato)ruthenium (II), sodium boranocarbonate, dimanganese decacarbonyl, and iron pentacarbonyl. Further disclosed are compositions and methods for treating a subject in need of a blood product by administering to the subject a composition including a CORM and a blood product (e.g., cryoprecipitate or fresh frozen plasma).
US20090233969 Biaryl substituted nitrogen containing heterocycle inhibitors of lta4h for treating inflammation The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
CN103549649A Health-care gum cigarette The invention discloses a health-care gum cigarette, and belongs to the field of novel tobacco products. The health-care gum cigarette is made of the following raw materials in percentage by weight: 0.001-0.2 percent of edible nicotine, 2-10 percent of green bonnie flower extract, 2-10 percent of sky-fruit extract, 40-60 percent of soybean oligosaccharides, 25-40 percent of gum base, 1-6 percent of menthol and/or fruit extract and 4-10 percent of sorbitol. The health-care gum cigarette has the advantages that (1) the product form is popular and fashion, and various styles are realized; (2) the health-care gum cigarette is convenient to carry and use, does not produce smog and can achieve the effect of freshening breath; (3) the health-care gum cigarette has the health-care effects of decreasing blood sugar, decreasing blood fat and lowering blood pressure.
US7776919 modulators of the interaction between the receptor for advanced glycated end products; 3-(4-Benzyloxyphenyl)propionic Acid 2,4- Di-(3-Diethylamino-1-propoxy)aniline Amide; acute and chronic inflammation; diabetic late complications; Alzheimer's disease, erectile dysfunction; metastasis This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
US20120115846 Quinazolinedione derivatives, preparation thereof and various therapeutic uses thereof. The subject matter of the invention is quinazolinedione derivatives of formula (I), methods for obtaining same and therapeutic uses thereof, such as cancer, diabetes, muscle diseases, bone diseases, cardiovascular diseases, central nervous system diseases, peripheral nervous system diseases, inter alia.
WO2006061309A1 Process for the preparation of drospirenone A process is described for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action; comprising the oxidation of 17α-(3-hydroxypropyl)-6β, 7β, 15β, 16β-dimethylene-5β-androstane- 3β , 5, 17β -triol.
EP1689411A2 Graduated estrogen contraceptive A multiphasic estrogenic/progestogenic contraceptive regimen that provides for the reduction or elimination of estrogen in the initial phase is disclosed. Also described is a contraceptive kit that may be used to practice the method of the invention.
CN102038695A Application of acarbose to preparation of medicament or feed for ruminants The invention discloses application of acarbose to preparation of a medicament or feed for ruminants, and in particular relates to application to preparation of a medicament or feed for increasing the pH value of a rumen and preventing or treating rumen acidosis of the ruminants. Due to the application of the acarbose, the rumen fermentation mode of a goat is changed; the pH value of the rumen is increased; and blood sugar in blood, cholesterol, triglyceride, blood urea nitrogen and serum total protein are not influenced obviously. In-vitro batched fermentation tests prove that the ph value during in-vitro fermentation is increased obviously and the gas production rate of rumen microorganisms within 24 hours is reduced after the acarbose is added. Due to the application of the acarbose, the rumen pH value of the ruminants can be effectively increased and rumen acidosis can be prevented or treated.
US8227404 Method of preventing acute or sub-acute hepatic failure in a subject by administering a soluble human tumor necrosis factor alpha fusion protein The present invention belongs to the field of the application of genetic engineering and gene function, and it is directed to a new medical use of the gene encoding the recombinant soluble tumor necrosis factor α receptor (HusTNFR). The present invention made intervention to fulminant hepatic failure in mice by use of the long-acting recombinant human soluble tumor necrosis factor α receptor and the classic animal models of acute and sub-acute hepatic failure. The results showed that the long-acting soluble tumor necrosis factor α receptor of the present invention has a half-life extended more than 10 times, and it significantly decreased the mortality of model animals and has superior therapeutic effect for the treatment and/or prophylaxis of acute and sub-acute hepatic failure in model animals. These receptors have a noticeable therapeutic effect for the treatment and/or prophylaxis of acute and sub-acute hepatic failure in comparison with the non-long-acting HusTNFR.
US20110212137 Inhalable pharmaceutical composition An inhalable pharmaceutical solution aerosol comprising beclometasone dipropionate, ethanol and a propellant selected from 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane and a mixture thereof, wherein the aerosol has a droplet size having a mass median aerodynamic diameter of 0.5-2.0 μm, for maintaining lung function above 60% of baseline FEV1, or reducing the occurrences of lung function falling below 60% of baseline FEV1.
CN101972259A Brucine and application of derivatives thereof in preparation of drugs for treating alcoholic abuse and dependence The invention relates to brucine, derivatives thereof and a new medical application of a brucine extractive. Particularly, the invention relates to brucine, derivatives thereof and an application of derivatives thereof in the preparation of drugs for preventing or treating alcoholic abuse and dependence.
CN101269022A Darifenacin hydrobromide sustained-release dropping pills and preparation method thereof The invention discloses a medicine composition oral preparation used for curing the disease symptoms such as overactive bladder along with symptoms of urge incontinence, urgency of micturition and frequency of micturition, more particular relates to a hydrobromic acid darifenacin sustained-release pill used for curing the diseases such as syphilis, gonorrhoea and chlamydia or mycoplasma infection, etc. The invention aims at making up the deficiency of the prior art and provides a hydrobromic acid darifenacin sustained-release pill. The hydrobromic acid darifenacin sustained-release pill related by the invention effectively overcomes the defects of the prior art and ensures that the medicaments do not have apparent quality change within the valid storing period, at the same time, the hydrobromic acid darifenacin sustained-release pill has the advantages of controllable medicine releasing time, enough medicine release and high bioavailability.
CN1823815A Application of sodium sulfide vein injection liquid in preparation of medicine for treating sequela of cerebral embolism death An application of the venous injection of sodium sulfide in treating the sequelae of cerebral infarction, such as aphasia, hemiplegia, dementia, etc, by suppressing the release of serozyme is disclosed.
WO2012020738A1 Heterocyclic compound and use thereof A compound that has agonist activity against GPR52 and that is useful as a preventive or therapeutic drug for mental disorders and the like such as schizophrenia is provided. The compound is a compound represented by general formula (I) [where each symbol is as defined in the Specification] or a salt thereof.
US20100184657 Methods of treating epithelial lesions outside the stomach and intestines Intestinal trefoil factors and nucleic acids encoding intestinal trefoil factors are disclosed. The intestinal trefoil factors disclosed are resistant to destruction in the digestive tract and can be used for the treatment of peptic ulcer diseases, inflammatory bowel diseases, and other insults.
US20130072568 Retinoid replacements and opsin agonists and methods for the use thereof Compositions of and methods for using synthetic retinoids as retinoid replacements and opsin agonists are provided.
US7615550 Such as 1-(4-{[1-(1-methylethyl)-4-piperidinyl]oxy}phenyl)-4-{[4-(methylsulfonyl)phenyl]carbonyl}piperazine; neurodegenerative disorders including Alzheimer's disease; allergic rhinitis The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.
US7807664 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or salt thereof A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.
US20130005704 Substituted arylimidazolone and triazolone as inhibitors of vasopressin receptors The present application relates to novel, substituted 4-arylimidazol-2-ones and 5-aryl-1,2,4-triazolones, processes for the production thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases and the use thereof for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.
US20120129893 Inhibition Of Raf Kinase Using Substituted Heterocyclic Ureas Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
US7547680 Benzimidazole derivatives and medical uses thereof The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R4 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.
CN103339139A 7-deazapurine modulators of histone methyltransferase, and methods of use thereof Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransf erases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.
EP1696904B1 Use of rotigotine for the treatment or prevention of dopaminergic neurone loss The invention relates to the use of rotigotine or salts thereof and prodrugs for the production of a medicament for the treatment or prevention of dopaminergic cell destruction in diseases which are connected to increased dopaminergic cell destruction. The invention also relates to the use of rotigotine as a medicament for the preventive treatment of Parkinson's disease.
US20070244108 Phenylsulfonamide Derivatives for Use as 11-Beta-Hydroxysteroid Dehydrogenase Inhibitors 1. A compound having Formula I R1—SO2NR3-L-R2 Formula I wherein R1 is an optionally substituted phenyl ring; R2 is a heterocyclic ring; R3 is H or a hydrocarbyl group; and L is an optional acyclic linker wherein when R2 is a five-membered aromatic heterocyclic ring, L is present.
CN102391287A Levo-fluoroquinolone C3 bisazole methyl sulfide, preparation method and application thereof The invention belongs to the technical field of medicine, and in particular discloses a levo-fluoroquinolone C3 bisazole methyl sulfide, a preparation method and application thereof in the field of pharmacy. The chemical structural formula of the levo-fluoroquinolone C3 bisazole methyl sulfide is shown as a general formula I, wherein in the general formula I, X is selected from any one of O, S and -NH; and Ar is selected from any one of phenyl, substituent-containing phenyl and heterocyclic aromatic hydrocarbon. The levo-fluoroquinolone C3 bisazole methyl sulfide has strong in vitro cytotoxin effect on experimental leukemia cancer cell strains, has strong anti-tumor activity, and can be mixed with a human acceptable acid salt or a medicinal carrier to prepare an anti-tumor medicament.
CN103156877A Capecitabine immediate-release pellet and preparation method thereof The present invention relates to a capecitabine immediate-release pellet and a preparation method thereof. The capecitabine immediate-release pellet includes the compositions of capecitabine, an excipient, a disintegrating agent and an adhesive. The particle size of the pellet is 0.1-10 mm. The extrusion granulator technology is used in the present invention to prepare the capecitabine immediate-release pellets and the pellets are directly filled into capsules, thus the production process is greatly simplified. The method is simple and reliable. The capecitabine immediate-release pellets prepared by the present invention are good in reproducibility and high in yield.
CN101759699B Pyrro-perhydroazepinone compound and application thereof in preparing medicaments for treating tumors The invention discloses a pyrrole-perhydroazepinone compound and an application thereof in preparing medicaments for treating tumors, aiming to provide a pyrrole-perhydroazepinone compound having the inhibiting effect on tumor cells and a structure of a formula (I) and medicinal salt thereof. The compound is expressed by the formula (I), wherein n represents 0 or 1; R1 represents H, a C1-C6 alkylgroup or a benzyl group; R2 represents OH or O; R3 represents H, a trifluoro-methyl, a C1-C6 alkyl group or OR4; and R4 represents H or a C1-C6 alkyl group.
CN1717252B Preparation containing basic drug The present invention provides a pharmaceutical preparation containing basic physiologically active substance and enteric polymer, which has improvements in releasability of the contained physiologically active substance in intestinal canal. The basic medicine-containing preparation of the present invention comprises one or more electrolytes by which the action of the enteric polymer to suppress release of the basic physiologically active substance is improved.
EP1609470A1 Nasal delivery of apomorphine Intranasal delivery methods and compositions for the delivery of dopamine receptor agonists are provided which are effective for the amelioration of erectile dysfunction in a mammal without causing substantial intolerable adverse side effects to the mammal. Nasally administered compositions for treating male erectile dysfunction in a mammal are also provided which include a therapeutically effective amount of dopamine receptor agonist which has been dispersed in a system to improve its solubility and/or stability.
EP2175865A2 Controlled release interferon drug products and treatment of hcv infection using same The invention relates to controlled release formulations comprising a microparticle comprising a biodegradable polymer and one or more interferon compounds and methods of using the formulations.
EP2062880A1 5-[(3,3,3-Trifluoro-2-hydroxy-1-arylpropyl)amino]-1H-quinolin-2-ones, a process for their production and their use as anti-inflammatory agents The present invention relates to compounds of formula I, processes for their production and their use as anti-inflammatory agents.
EP1248841B1 Genes differentially expressed in breast cancer A polynucleotide sequence as shown in SEQ ID NO:1 is associated with metastatic potential of cancer cells, especially breast cancer cells. Methods are provided for determining the risk of metastasis of a tumor, by determining whether a tissue sample from a tumor expresses a polypeptide or mRNA encoded by a polynucleotide as shown in SEQ ID NO:1. Also provided are therapeutic methods and compositions.
CN103059045A Novel amoxicillin sodium and clavulanate potassium compound and pharmaceutical composition thereof The invention discloses a novel amoxicillin sodium compound. The purity of the amoxicillin sodium compound is more than 99.5%. Meanwhile, the invention also discloses a pharmaceutical composition of an amoxicillin sodium and clavulanate potassium compound. The pharmaceutical composition comprises the following components in parts by weight: 200-400 parts of amoxicillin sodium, 20-36 parts of potassium clavulanate, 1-18 parts of propyl cellulose and 0.2-8 parts of collagen. According to the pharmaceutical composition of the amoxicillin sodium and potassium clavulanate compound, a synergistic effect is generated between propyl cellulose and collagen, so that a slow-release period of an amoxicillin sodium and potassium clavulanate formulation reaches as long as 24 hours, the amoxicillin sodium and potassium clavulanate formulation can be administered once one or two days, thus a patient takes medicine conveniently.
EP2460518A1 Composition including a chondroprotective agent and vitamins Composition (I) comprises at least one chondroprotective element comprising glucosamine and its derivatives and chondroitin sulfate and its derivatives, vitamin C and vitamin D. - ACTIVITY : Anabolic; Antirheumatic; Antiarthritic; Osteopathic; Analgesic; Antiinflammatory. - MECHANISM OF ACTION : None given.
US20070185174 Use of thiazole derivatives for preparing a medicament intended to protect the mitochondria A method of treating Leber's syndrome in warm-blooded animals in need thereof an effective amount of a compound of the formula where the substituents are defined as in the specification.
WO2013133873A3 Pharmaceutical compositions of sodium ion and calcium ion and methods for treating cancer, tumor and non-malignancy The invention relates to a unique formulated pharmaceutical composition and a novel treatment method of intratumoral injection. The pharmaceutical composition of the invention is the saturated ionic solution of sodium ions and calcium ions (the "medicinal ion bomb"). The invention of intratumoral injection with the "medicinal ion bomb" can be used as the first-line treatment in treating cancer and tumor in nine human organs (carcinoma and tumor of the skin and subcutaneous tissue, breast, prostate, thyroid, lung, liver, genital organ, brain and pancreas) and certain other benign diseases (skin and subcutaneous neoplasm, breast fibrocystic change, benign prostatic hyperplasia and thyroid nodules).
WO2009096526A1 Carboxylic acid compound or salt thereof Provided is a compound having a CRTH2 antagonism and being useful as a preventive and/or remedy for inflammatory diseases (for example, asthma, allergic rhinitis, allergic dermatitis, conjunctivitis, urticaria, eosinophilic bronchitis, food allergy, sinusitis, angiitis, chronic obstructive pulmonary disease, etc.) or multiple sclerosis. As the results of studies on compounds having a CRTH2 antagonism, it has been confirmed that a carboxylic acid compound or a salt thereof has a CRTH2 antagonism. The above-described carboxylic acid compound or a salt thereof has a CRTH2 antagonism and is usable as a preventive and/or remedy for inflammatory diseases (for example, asthma, allergic rhinitis, allergic dermatitis, conjunctivitis, urticaria, eosinophilic bronchitis, food allergy, sinusitis, angiitis, chronic obstructive pulmonary disease, etc.) or multiple sclerosis.
US20050260277 Method and formula for anti-tumor and anti-matastatic effect The invention discloses an expeditious method and formula for treating cancer patients that reaulst in tumor suppression and remission, the suppression of mobilization and adhesion of cancer cells, and repression of pathogens, such as infectious bacteria and viruses. Administration is by oral ingestion or direct injection into tumors or intravenous drip etc. The invention employs control of intracellular and extracelular ionic physiology by administering alkaline salts, thereby restoring localized and/or systemic cellular ionic physiology, depriving cancerous cells of their ability to grow rapidly, and simultaneously normalizing their local environment, thereby inhibiting angiogenesis, enabling immune responses, and simultaneously reducing pain. The method further promotes correction of acidotic conditions often associated with cancer and other diseases, thereby potentiating biological functions of immunity and repair.
EP1986657A2 Method of treating a subject suffering from degenerative disc disease using a matrix metalloprotease inhibitor The present invention provides a method for treating a vertebrate subject suffering from a degenerative disc disease by administering an inhibitor of a matrix metalloprotease (MMP) to the subject in an amount effective to treat, the subject.
EP2393802A1 Dihydroquinolinone derivatives The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. A dihydroquinolinone derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: [Formula 1] {wherein Q represents the following formula (A) or (B)} [Formula 2]
WO2006035459A1 An improved process for the production of derivatives of thiozolidinediones and their precursors The invention provides a process for preparing derivatives of thiozolidinediones and their precursors comprising, (a) reacting a compound of general formula I wherein R1, R2 and R3 may be same or different and represent H, alkyl or alkoxy with C varying from 1 to 6, halogens, mono or di-substituted alkyl and aryl amines, and M represents hydrogen (H) or alkali metal selected from Na, K or Li with a compound of formula II, wherein R4 has the same meaning as R1 or R2 or R3 and X is halogen in presence or absence of solvent(s) under effective conditions to produce nitro ethers of general formula III, where in R1 to R4 has the same meaning as given above, provided when M is H and not its alkali metal salt, an alkali metal salt such as hydroxide or carbonate is required to be added while conducting the said reaction, (b) subjecting the said nitro ethers, with or without isolation, to Raney nickel-catalyzed reduction under conditions effective to produce corresponding nitro aniline ethers (c) coupling the said aniline ether with acrylates under Meerwein arylation conditions in presence of hydrobromic acid to produce α bromo substituted carboxylic acid derivatives followed by subjecting to solvent extractive purification (d) cyclising the purified derivative of α bromo substituted carboxylic acid as obtained in step (c) with thiourea to yield 2-imino -4-thiazolidinones then (e) hydrolyzing the said 2-imino-4-thiazolidinones to produce 2, 4-thiazolidinones and converting the same to its hydrochloride salts as white crystalline solids known to exhibit antidiabetic activity, by conventional methods.
CN101785773A Use of metal supermolecular compound in preparation of medicament for treating alzheimer's disease The invention relates to the technical field of supermolecular compounds and discloses the use of the metal supermolecular compounds in the preparation of the medicament for treating alzheimer's disease. The core metal ions of the metal supermolecular compound are all Ni<2+>s or Fe<2+>s; the ligands of the metal supermolecular compound have a molecular formula of C25H20N4. In a mole of the metal supermolecular compound, two metal positive ions and three imine-based ligands are bonded by coordinate bonds; and the Fe<2+>s and the N form a stable hexa-coordinate structure or the Ni<2+>s and the N form a stable hexa-coordinate structure so as to form a double-core metal three-spiral cylinder structure. The central phenylene surfaces of the metal supermolecular compound interact with the aromatic branch chains of the A beta amino acid residues through hydrophobic effect and the action of Pi bonds. The charge parts at two ends of each mole of the metal supermolecular compound can be bonded with the A beta amino acid residues by electrostatic interaction so as to inhibit the aggregation of the A beta amino acid residues.
CN102250186A Berberine-oryzanol compound, and preparation method and application thereof The invention belongs to the technical field of pharmaceutical synthesis, and particularly relates to a berberine-oryzanol compound having a structure shown in formula (I), and a preparation method and application thereof. In the invention, oryzanol (3) and berberine derivates (2) used as initial reactants are subjected to linking reaction under proper conditions, thus obtaining a berberine-oryzanol compound (1). After going into a human body, the compound is stable in the stomach; and after going into the intestinal tract, the compound can be resolved into berberine derivates and oryzanol in the alkaline environment to produce a medication effect. The compound has high fat solubility and good absorption performance. The compound can be further prepared into medicaments for treating cardiovascular diseases, especially medicaments for treating metabolic syndromes. The synthesis method has the advantages of simplicity and low price, and can be easily industrialized, thereby having very good prospects.
CN101108835A Method of manufacturing high purity hydrochloric acid sarafloxacin A preparation method of the sarafloxacin hydrochloride with high purity is provided. The sarafloxacin hydrochloride uses the 2, 4-dichlorofluoroacetophenone as raw material and becomes the 7-chlorine-6-fluorin- p-fluoro phenyl-1, 4- oxo-quinoline-3-hydroxy acid through etherification, ammonification, cyclization and hydrolysis, and then is condensed with the piperazine and reacts with the dry hydrogen chloride to become salt after refining. When in detailed preparation, the isoamyl alcohol of 400g is added in a reactor of 3L and stirred, added with piperazine anhydrous of 95g and salad carboxylic acid of 100g, and keeps reflux for 6h, recovers the isoamyl alcohol by decompression and steams up the isoamyl alcohol, and is added with water of 1.5L and added with sodium hydroxide to adjust the pH value not less than 12, and is hydrolyzed for 0.5h and filtered when heating to adjust the pH equal to 6.5-7.0, and is crystallized, filtered and added with purified water of 800g and active carbon of 5g, and keeps the reflux for 0.5h and is insulated and performs pressure filtration, and is rinsed, dried, added with methylene chloride of 1.2kg and stirred and is connected with dry hydrogen chloride until no crystal produces.
US20110034489 Solid dosage forms of hiv protease inhibitors The present invention relates to a solid dosage form comprising a solid dispersion composition of at least one HIV protease inhibitor and water soluble polymer having a glass transition temperature (Tg) of at least about 50° C. in an amount of less than 50% by weight of the dosage form. It also relates to a process of preparation of such solid dosage forms.
CN101175495B Anti-cancer compound combination The present invention relates to a therapeutic combination of anti-cancer compounds which comprises a) a VEGFR-2 inhibitor, and b) a substance that binds to the epidermal growth factor receptor (EGFR) and blocks the ability of epidermal growth factor (EGF) to initiate receptor activities which results in tumor growth inhibition, and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use.
US20100113511 Mono Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.
US6923988 Solid carrier includes a hydrophililc surfactant and a drug The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutritional agents, cosmeceuticals and diagnostic agents.
EP1335726B1 Modified prodrug forms of ap The present invention relates to compounds according to the structure of following formula (I), where R is H or CH3; R2 is phosphate which can be free acid or salt; R3 is H, F, C1, Br, I, OCH3, OCF3, CF3 or a C1-C3 alkyl group; R4 is H, F, C1, Br, I, OCH3, OCF3 or CF3; and R5 and R6 are each independently H, F, C1, Br, I, OCH3, OCF3 or CF3, with the proviso that when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H which may be used to treat neoplasia, including cancer.
WO2014084744A1 Saccharide dendritic cluster compounds as inhibitors of bace-1 The invention relates to dendritic compounds, the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, processes for preparing the compounds, and methods of treating diseases or conditions in which it is desirable to inhibit β-secretase.
CN101284780A 5-position acylated shikimic acid or low-carbon alcohol ester thereof, preparation and applications thereof The invention designs and synthesizes 5-acylated shikimic acid or low carbon alcohol ester thereof. The shikimic acid is a natural product with the biological activity, and has the effects of anti-thrombosis and reducing the injury of local cerebral ischemia. Because the polarity is large, the shikimic acid is not easy to be absorbed through oral administration, the synthesis of the single acidated derivant, the conditioning of the polarity, the increasing of the fatsoluble and the penetrating capacity of the blood brain barrier are significant; the 5-acylated shikimic acid or the low carbon alcohol ester thereof can be the compound with the unique biological activity, and can be developed into a novel medicine. Simultaneously, because the 5-acylated shikimic acid or the low carbon alcohol ester thereof perfectly keeps the three chiral centers of the shikimic acid structurally, the 5-acylated shikimic acid or the low carbon alcohol ester thereof is a starting material and intermediate which are synthesized through available chiral medicine. In addition, the 5-acylated shikimic acid or the low carbon alcohol ester thereof inherently has the surface activity, which can be used as the surface active agent to be applied to the medical field, the food field and the daily cosmetic field.
US20110190368 Organosulfur Compounds, a Method of Making Organosulfur Compounds and their Use for Inhibiting the Growth of Tumour Cells Organosulfur compounds of the general formula (2) are described, wherein R1 and R2 are linear or branched C1-C5 alkyl; linear or branched C1-C5 alkenyl with the proviso that R1 is not prop-1-enyl (allyl); substituted linear or branched C1-C5 alkenyl or substituted linear or branched C1-C5 alkyl, in which the substituents are selected from OR3, NR4R5, COOR6, CON—R7R8, in which R3 is selected from H, COR9, para-methoxybenzyl and trialkylsilyl, in which R9 is alkyl or substituted alkyl; R4 N and R5 are alkyl or R4 and R5 together form a phthalimido group; R6 is alkyl or substituted alkyl; and R7 and R8 are alkyl or substituted alkyl; substituted or unsubstituted aromatic specifically where R1 and R2 are benzyl, para-methoxybenzyl and/or ortho,para-methoxybenzyl and substituted or unsubstituted heteroaromatic. The compounds can be used for inhibiting the growth of tumour cells and for treating cancer. A pharmaceutical composition and a method of preparing the compounds are also described.
CN103446587A Application of mastocyte inhibitor in preparation of medicine for resisting influenza virus infection The invention discloses an application of a mastocyte inhibitor in the preparation of a medicine for resisting influenza virus infection. According to the application disclosed by the invention, the pivotal role of the mastocyte in the influenza virus infection is firstly proved, the curative effect of the existing medicine for resisting the influenza virus infection can be obviously improved by taking the advantage of the mastocyte inhibitor, and therefore a medicine composition for treating the influenza is provided.
WO2003103643A8 Oral antidepressant formulation comprising a selective serotonin_reuptake inhibitor Oral antidepressant formulation comprising an effective antidepressant amount of one or more selective serotonin reuptake inhibitors, and an effective amount of at least a compound selected from the group consisting of acetylsalicylic acid, derivatives of acetylsalicylic acid, heparin, heparin like compounds, and mixtures thereof, for reducing the onset of action of the selective serotonin reuptake inhibitor(s).
US7323563 Hydroxamic acid derivatives as antibacterials A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:
US20090082335 Deuterium-enriched oxcarbazepine The present application describes deuterium-enriched oxcarbazepine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN101972245A Composition capable of promoting insulin secretion and inhibiting generation of advanced glycosylation end products The invention relates to a composition capable of promoting insulin secretion and inhibiting generation of advanced glycosylation end products. The composition comprises the following components in percentage by mass: 5-95% of proanthocyanidin extract and 5-95% of dihydrochalcone. The main component of the proanthocyanidin extract is proanthocyanidin which accounts for 50-70% of the mass of the extract. The composition lays a foundation for the production of the future compound medicines, is beneficial to controlling blood sugar of diabetics and preventing and treating diabetic complications. The composition of the invention has the advantage that the multifunctional synergistic effect is obviously superior to effect of each independently used component.
CN102861155A Cream for treating psoriasis The invention relates to a cream for treating psoriasis, wherein the constituents of the cream are as follows: flos lonicerae, balsamine, radix sophorae flavescentis, cortex dictamni, fructus cnidii, rhizoma coptidis, olibanum, borneol, cream and the like. The product is externally applied and health-care, and has the health care effects for promoting the skin irritations caused by psoriasis, tigason, eczema, dermatitis and insect bites and the like. The cream for treating psoriasis is approximately applied to the uncomfortable parts when the cream is utilized and then is penetrated after waiting for 1 to 2min. The cream provided by the invention is prepared by the natural medicinal raw materials, any chemical harmful substance is not added, the efficacy is ideal, and the cost is low, so that the cream for treating psoriasis is suitable for popularization and application.
CA2592407A1 Methods of treating pain The present invention is directed to methods and compositions for inducing, promoting or otherwise facilitating pain relief. More particularly the present invention discloses the combination of a nitric oxide donor and an opioid analgesic in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, particularly moderate to severe pain. In particular, the nitric oxide donor is a slow-release nitric oxide donor or is formulated to provide a sustained release of a low dose of nitric oxide.
CN103145726A Longikaurin A as well as medicinal composition and application thereof The invention belongs to the field of medicines, and in particular relates to longikaurin A which is extracted and separated from isodon ternifolius and is as shown in the structural formula (I), as well as a medicinal composition and an application of the longikaurin A. In vitro anti-tumor activity screening shows that the longikaurin A shows strong inhibitory activity to experimental cell strains (SMMC-7721 and HepG2) of liver cancer and experimental cell strains (CNE1 and CNE2) of nasopharyngeal cancer. The longikaurin A can be singly applied to the preparation of medicines for resisting the liver cancer and nasopharyngeal cancer, and can also be used for forming various preparation types and medicinal compositions of the medicines for resisting the liver cancer and nasopharyngeal cancer with other medicinal adjuvant materials.
WO2010004319A1 Combination comprising 6-flu0r0-n- ((1s, 4s) - 4- (6-fluoro-2, 4-di0x0-1- (4'- (piperazin-1- ylmethyl) biphenyl- 3-yl) -1, 2-dihydropyrido [2, 3-d] pyrimidin-3 (4h) - yl) cyclohexyl) imidazo [1,2-a] pyridine -2- carboxamide or a salt The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is 6-fluoro-N-((1s,4s)-4-(6-fluoro-2,4-dioxo-1-(4'-(piperazin-1- ylmethy1)-biphenyl-3-yl)-l,2-dihydropyrido[2,3-d]pyrimidin-3(4H)- yl)cyclohexyl)imidazo[l,2-a]pyridine-2-carboxamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a β2 adrenoceptor agonist; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; a MABA compound; an MPO inhibitor; a muscarinic antagonist; a p38 inhibitor; a PPARγ agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
CN101880304A 24(R)-pseudoginsenoside-GQ as well as semisynthesis method and medicinal application thereof The invention relates to 24(R)-pseudoginsenoside-GQ as well as a semisynthesis method and medicinal application thereof, belonging to a new compound as well as a synthesis method and medicinal application thereof. In the invention, 20(S)-ginsenoside Rg3 or 20(R)-ginsenoside Rg3 is used as a raw material, and under an acid condition, a new compound is synthesized through the steps of oxidization, cyclization, and the like, wherein the chemical name of the new compound is 3-O-[beta-D-glucopyranose-(1-2)-beta-D-glucopyranose group]-damma-20S, 24R-epoxy-3beta, 12beta, 25-triol being short for 24(R)-pseudoginsenoside-GQ, the productivity of which reaches higher than 80 percent. The 24(R)-pseudoginsenoside-GQ has wide medicinal application in preparing medicaments for treating coronary heart diseases, myocardial ischemia, ischemic shocks, arrhythmia and reperfusion damages and resisting cancer.
CN1903308B Active position of Omithogalum caudatum ait, its preparation method, medicine and application thereof An active part of ornithogalum is prepared through extracting from ornithogalum to obtain liquid extract, centrifugal separation of impurities, recovering solvent, concentrating and freeze-drying to obtain powder. It can be used to prepare the medicine for treating tumor.
CN203107746U Aspirin dipyridamole slow-release structure The utility model relates to an aspirin dipyridamole slow-release structure, which comprises a dipyridamole layer 1, an isolation layer 2, an aspirin layer 3 and a protective layer 4 successively from inside to outside. According to the utility model, as the isolation layer is arranged between the dipyridamole layer and the aspirin layer, the situation that the dipyridamole layer and the aspirin layer contact each other to result in generation of aspirin degradation product salicylic acid can be prevented; and the protective layer is arranged outside the aspirin layer, and can effectively prevent aspirin from interacting with outside moisture, thus reducing aspirin degradation rate.
CN102127037A Tanshinone compounds and applications thereof The invention relates to tanshinone compounds in the technical field of medicine and applications thereof. The tanshinone compounds contain tanshinone I, tanshinone IIA, cryptotanshinone and dihydrotanshinone I and the structural formulas are shown as below. The method of the invention uses the tanshinone compounds as the active ingredients of the androgen receptor antagonist; the compounds are used alone or used along with the excipient to prepare oral agents or non-oral agents for curing the diseases related to androgen.
US20080200515 Solid state forms of enantiopure ilaprazole The invention relates to solid state forms of enantiopure ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfnyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a solid form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders such as those discussed above.
CN101095751A Medicinal composition having functions of removing chloasma and improving nutritional anemia and method for preparing the same The invention provides a pharmaceutical composition for dispelling snuff brown speckles and treating trophism hyphemia, the process for preparation and quality control method thereof, wherein the composition is prepared from seabuckthorn fruit, wolferry fruit, Chinese angelica root, safflower, pilose asiabell root, Cinnamomum cassia, pearl powder and chlorinated ferriheme through steps of disintegrating safflower, Cinnamomum cassia, pearl powder and chlorinated ferriheme into fines, charging water into seabuckthorn fruit, wolferry fruit, Chinese angelica root and Codonopsis pilosula, concentrating, drying, mixing the obtained concrete powder with the fines of medicinal material homogeneously to obtain conventional preparations.
EP1860101A1 Tartrate sale of isofagomine and methods of use A novel tartaric acid salt of Isafagomine (Isofagomine tartrate) that can be used for the treatment of Gaucher disease is provided. The invention also provides a crystalline form of isofagomine tartrate, method for preparing the salt, a pharmaceutical composition containing the salt, and a method of treating Gaucher disease.
WO2008131858A3 Use of acyclically substituted furopyrimidine derivatives for treating pulmonary arterial hypertonia The invention relates to the use of acyclically substituted furopyrimidine derivatives of formula (I) for the treatment and/or prophylaxis of pulmonary arterial hypertonia and other forms of pulmonary hypertonia and to the use of said derivatives for producing medicaments for the treatment and/or prophylaxis of pulmonary arterial hypertonia and other forms of pulmonary hypertonia.
US6949545 Tissue remodeling; antiinflammatory agents; autoimmune disease Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R1, R2, R3, n, A, E, X, G, G′, M and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
WO2013121440A1 Process for preparing benzisothiazol-3-yl-peperazin-l-yl-methyl-cyclo hexyl-methanisoindol-1,3-dione and its intermediates The present invention discloses process for preparing benzisothiazol-3-yl- piperazin-l-yl-methyl-cyclo hexyl-methanisoindol-l,3-dione and intermediates thereof.
CN101023943A Myricetin dispersion tablets for treating cardio-cerebral blood vessel diseases The present invention discloses a myricetin dispersion tablet for curing angiocardiopathy and cerebrovascular disease. Its composition contains (by weight portion) 100-200 portions of myricetin or myricetin containing 2% of borneol, 10-35 portions of cross-linked polyvinylpyrrolidone, 40-150 portions of microcrystal cellulose, 40-80 portions of alpha-lactose or 50-150 portions of pregelled starch, 10-35 portions of polyvinylpyrrolidone, 1-10 portions of sodium lauryl sulfate and 1-5 portions of magnesium stearate. Said invention also provides the preparation method of said dispersion tablet.
CN101095672A Novel pharmacy use of medicinal composition The invention discloses the novel use of four kinds of medicinal compositions of catechin in preparing pharmaceuticals, the antineoplastic preparation prepared from a specific proportion of the catechin pharmaceutical compositions has better therapeutic effects.
CN101225146A Chitosan-ketoprofen grafts and preparation method thereof The invention rglates to chitosan-ketoprofen grafted substance and the preparation method, belonging to pharmacy field, which can be grafted on the framework of degradable macromolecular material chitosan to make polymer medicine. The preparation method adopts the degradable macromolecular material chitosan to structure qualify the ketoprofen and uses the 1- (3-dimethylaminopropyl)-3-ethyl carbodiimide hydrochloride as the catalyst, and then accelerates the chitosan and the ketoprofen to connect by the amido links to compose chitosan-ketoprofen grafted substance. The chitosan-ketoprofen grafted substance can be used in curing the arthritis and prolonging the medicine acting time when adopting the injection medication. The preparation method for the chitosan-ketoprofen grafted substance also has the advantages of simple preparation method, easy operation and good reproduction quality.
CA2814696A1 Pharmaceutical formulation for histone deacetylase inhibitors A pharmaceutical composition, comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound represented by the following structural formula at least one acidifying agent; and a vehicle base comprising at least one pharmaceutically acceptable non-aqueous solvent. Values and preferred values of the variables in structural formula (I) are defined herein.
US20060025484 Use of 1-(2-chloroethyl)-1-nitroso-3-(2-hydroxyethyl)urea for treatment of pancreatic carcinomas, soft tissue sarcomas, testicular tumors, lymphomas, thymomas, wilms' tumors, renal carcinomas, melanomas, lung tumors, intracerebral metastases, tumors in the head and neck area and mammary carcinomas This invention relates to the use of 1-(2-chloroethyl)-1-nitroso-3-(2-hydroxyethyl)urea (hereinafter also referred to as HECNU) for treatment of pancreatic carcinomas, soft tissue sarcomas, testicular tumors, lymphomas, thymomas, Wilms' tumors, renal carcinomas, melanomas, lung tumors, intracerebral metastases, tumors in the head and neck area and mammary carcinomas.
CN101085089A Gargle medicine for treating stomatocase The invention discloses a gargle medicament for treating ulcerative stomatitis, wherein the active constituents include the following raw material herbs (by weight portion): baikal skullcap root 20g, phellodendron bark 20g, coptis root 10g, cape jasmine 15g, honeysuckle flower 15g, peppermint 10g, licorice root 6g, borneol 3g. The preparing process consists of mixing baikal skullcap root, corktree bark, goldthread root, cape jasmine, honeysuckle flower, peppermint and licorice root, immersing in water for half a hour, loading into container and charging water 500ml, grilling for half a hour, charging borneol into the soup and homogenizing.
CN102784124A Cefuroxime axetil composition freeze-dried orally disintegrating tablets and preparation method thereof The invention provides cefuroxime axetil composition freeze-dried orally disintegrating tablets and a preparation method of the orally disintegrating tablets, relates to the field of a medicine and a medicine preparation method technology and mainly solves the problems in the prior art that the cefuroxime axetil preparation is poor in curative effect and not suitable for children and the patients who are difficult to swallow. The cefuroxime axetil composition freeze-dried orally disintegrating tablets are prepared from the following components by weight: 25-50% of cefuroxime axetil, 25-75% of mannitol, 2-4% of gelatin, 0.1-0.15% of trichlorosucrose and 42-67% of tertiary butanol-water. The cefuroxime axetil composition freeze-dried orally disintegrating tablets prepared by the above components are easy in preparation process, and simple in components, and mainly meet the administration requirements of children and the patients who are difficult to swallow; moreover, the cefuroxime axetil composition freeze-dried orally disintegrating tablets have the advantages of being fast to disintegrate, convenient to take, and good in taste; and the tablets take effect quickly and are fully absorbed, and the first pass effect of the liver is avoided.
US7361679 Integrin VLA-4 ( alpha 4 beta 1) and/or integrin LPAM-1 ( alpha 4 beta 7) antagonists, cell adhesion inhibitor; bioavailability, oral administration;treating inflammatory diseases; e.g. 3-[2-(2,6-dichlorobenzoylamino)pyrid-5-yl]-2-{3-[(2,2-dimethylpropionyl)isobutylamino]-4-methoxyphenyl}propionic acid The present invention relates to a 2-phenyl-3-heteroarylpropionic acid derivative or a salt thereof, and also relates to a pharmaceutical agent and a VLA-4 and/or LPAM-1 antagonist each of which contains the same as an active ingredient.
US7087743 Bleaching; skin disorders; genetic engineered nucleic acid; topical applying The present invention relates to novel oligonucleotide sequences and also to derivatives thereof. These novel oligonucleotide sequences are capable of hybridizing specifically with the gene or with a product of the gene encoding tyrosinase, or with the gene or a product of the gene encoding tyrosinase-related-protein 1 (TRP-1). The present invention also relates to the use of these novel oligonucleotide sequences as a depigmenting or bleaching agent in a cosmetic composition or in a dermatological composition.
WO2013067277A1 Alkylated piperazine compounds as inhibitors of btk activity Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
CN101564482B Compound liniment for treating acne rosacea The invention provides a compound liniment for treating acne rosacea, which consists of the following raw materials by weight percentage: cyproheptadine, vitamin B6, sulfur, mercurous chloride, radix sileris, clove oil, borneol and the like. The compound liniment accords with the chemical characteristics of skin, is advantageous for giving play to physiological functions of the skin, is safe and reliable for treating the acne rosacea, can quickly deliver drugs to a pathologic change part to diminish inflammation, kill mites and sterilize powerfully, and play a direct action on the root of niduses to thoroughly dispel symptoms of itching, red, blains and the like of the acne rosacea. By combining with DS reparative factors, the compound liniment can repair the microcirculation of the skin in a short time, regulate sebum secretion metabolism, and reconstruct the immunologic function of normal skin to thoroughly cure the acne rosacea and prevent recurrent attacks; and in the using process, the compound liniment reduces the dryness and tension of nose skin, has small acrimony, can be accepted by patients easily, and has broad application prospect.
US20110015155 Deuterated 2, 4-Pyrimidinediamine Compounds and Prodrugs Thereof and Their Uses The present disclosure provides biologically active deuterated 2,4-pyrimidinediamine compounds and prodrugs thereof, compositions comprising the deuterated compounds, intermediates and methods for synthesizing the deuterated compounds and methods of using the deuterated compounds in a variety of applications.
WO2013190508A3 1-[m-carboxamido(hetero)aryl-methyl]-heterocyclyl-carboxamide derivatives The present invention relates to 1-[m-carboxamido(hetero)aryl-methyl]-heterocycyl- carboxamide compounds of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5a, R5b and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
CN102123732A Compositions, methods and kits for eliciting an immune response The present invention relates to compositions, methods, and kits for eliciting an immune response to at least one CMV antigen expressed by a cancer cell, in particular for treating and preventing cancer. CMV determination methods, compositions, and kits also are provided.
US20080249111 Piperdine Derivatives as CCR5 Inhibitors Disclosed are compounds of formula I: wherein R1, R2, R3 and X are as defined herein, in free or salt form, which are useful as CCR5 inhibitors, e.g. in the prevention or treatment of disorders mediated by interactions between chemokine receptors and their ligands.
US8093227 Monosaccharide compounds and methods therefor A monosaccharide compound of formula I as shown in the specification. Processes for the preparation of the compound of formula I and methods of screening for antibacterial or antibiotic compounds involving the compound of formula I.
US20130011417 Colchicine derivatives or pharmaceutically acceptable salts thereof, method for preparing said derivatives, and pharmaceutical composition comprising said derivatives The present invention relates to colchicine derivatives expressed in chemical formula 1, or to pharmaceutically acceptable salts thereof, to a method for preparing said derivatives, and to a pharmaceutical composition comprising said derivatives. The colchicine derivatives according to the present invention exhibit superior immunomodulatory effects as compared with conventional immunomodulators or colchicines, and therefore can be valuably used as an immunomodulator for modulating an acute or chronic immune response in organ transplantation.
CN103721223A Medicine for treating functional uterine bleeding and preparation method thereof The invention discloses a medicine for treating functional uterine bleeding and a preparation method thereof. The medicine is mainly prepared from concha ostreae, fluorite violet quartz, herba ecliptae, turtle shell, folium mori, cockscombs, herba agrimoniae and other medicines according to a certain weight proportion. The medicine has the functions of cooling blood, stopping bleeding, dispersing blood stasis, relieving pain, calming the adverse-rising energy and warming the uterus, is high in efficiency when being used for treating functional uterine bleeding, and good in curative effect, and avoids relapse.
US20080280981 Oral dosage form; controlling blood concentration; urogenital disorders; edema; blood coagulation disorders in patient undergoing dental surgery Disclosed are oral tranexamic acid formulations and methods of treatment therewith.
WO2006024958A3 Cannabinoid compositions and methods of use thereof The present invention provides cannabinoid compositions and the use of such cannabinoid compositions in the treatment of autoimmune and/or inflammatory diseases and disorders. For example, the present invention provides a method of using tetrahydrocannabinoid (THC) compounds in the treatment of autoimmune and/or inflammatory diseases and disorders.
US20110130390 Use of COX-2 Inhibitors for the Treatment of Schizophrenia, Delusional Disorders, Affective Disorders, Autism or Tic Disorders The invention concerns the use of a COX-2 inhibitor for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders, in particular chronic schizophrenic psychoses and schizoaffective psychoses, temporary acute psychotic disorders, depressive episodes, recurring depressive episodes, manic episodes and bipolar affective disorders. Moreover, the invention is concerned with the use of a COX-2 inhibitor, in particular celecoxib, in combination with a neuroleptic drug, in particular risperidone, or an antidepressant, for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders.
EP2422790A1 Paramyxovirus family inhibitors and methods of use thereof The present invention provides compounds for the treatment of measles.
CN103505427A Agomelatine tablet The invention relates to an agomelatine tablet and a preparation method thereof, belonging to the technical field of medicines. The technical scheme of the invention is as follows: a unit dosage of tablet contains a VII type crystal of agomelatine, lactose, starch, sodium carboxymethyl starch, povidone (K30), stearic acid, magnesium stearate, silica and opadry.
CA2439838C (2-hydroxy)ethyl-thioureas useful as modulators of alpha2b adrenergic receptors Compounds of formula (i) and of formula (ii), wherein the symbols have the meaning disclosed in the claims, specifically or selectively modulate .alpha.2A adrenergic receptors and as such are useful for alleviating chronic pain and allodynia and have no or only minimal cardiovascular and/or sedatory activity. The invention also relates to a method of activating .alpha.2B or .alpha.2C adrenergic receptors in a mammal by administering a compound that has .alpha.2Bor .alpha.2C adrenergic receptor activity and has no significant .alpha.2A agonist activity.
CN103372162A Plaster for treating femoral head necrosis The invention relates to a plaster for treating femoral head necrosis. Each serving of the plaster for treating avascular necrosis comprises the following raw materials by weight: 7-9g of centipede, 25-30g of lumbricus, 5-10g of long-noded pit viper, 15-20g of baiyao, 25-30g of malt, 15-20g of bighead atractylodes rhizome, 15-20g of borneol, 25-30g of root of three-nerved spicebush, 10-15g of pseudo-ginseng, 5-10g of myrrh, 5-10g of musk and 0.5-0.6kg of liquor. The plaster for treating femoral head necrosis is convenient to use, and has obvious effect.
US20080279822 Crystalline Polymorphs of a CXC-Chemokine Receptor Ligand The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: Compound A. These four polymorphic forms, herein referred to as Forms I, II III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
WO2014077409A1 Agent for mitigating side effect of sunitinib The present invention relates to a method for mitigating a side effect of sunitinib by using the sunitinib and an antioxidant jointly with each other. It was discovered that the side effect of sunitinib is caused by an increase in oxidative stress and blood glycogen, and it was found that the side effect is mitigated by using an antioxidant jointly with the sunitinib.
US20130005687 Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of trpv1 Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
EP2358724A1 Tiotropium bromide having a low degree of crystallinity The present invention provides tiotropium bromide having a low degree of crystallinity. The present invention also provides a complex of tiotropium bromide and polyvinylpyrrolidone, processes for preparing it and pharmaceutical formulations including it.
CN103652926A Food composition for tumor patients The invention provides a food composition for tumor patients. The food composition consists of poria cocos, colla corii asini, dark plum, galangal, radix angelicae, peach kernel, liquorice, barbary wolfberry fruit, glossy privet fruit, lily, rhizoma polygonati, radix polygonati officinalis, Chinese yam, colla corii asini, longan aril, semen armeniacae amarae, Chinese date, hawthorn, clove, dandelion, sea cucumber, bean pulp and nutrient supplement selenium, wherein each component contains a plurality of anticancer factors with different functions; several components further have the effects of reducing blood pressure, blood sugar and blood fat. Except for the conventional nutrients and the plurality of anticancer factors of protein, fatty acid, polysaccharide, dietary fiber, mineral substance and vitamin, the food composition further contains a plurality of components with such pharmacologic actions as qi supplement, blood replenishment, stomach invigoration, spleen protection, spleen and stomach warming, cold dispelling, damp clearing, diuresis promotion, cough relieving, sputum reduction, adverse-rising energy calming, vomiting prevention, heat clearing and poison removal. The food composition for the tumor patients can exert the synergic effect of the anticancer factors in all the components to the greatest degree through the reasonable composition so as to help the tumor patients to prevent and resist cancers, and can comprehensively satisfy the dietary therapy demands and recovery conditioning of the tumor patients. All the selected components are edible materials without toxic or side effects on human bodies, and can be eaten for a long time.
WO2013029723A1 Novel photoactivatable paclitaxel derivatives and uses thereof, in particular in cellbiology and cancer treatment The present invention provides novel photoactivatable paclitaxel derivatives wherein the C2 and C7 positions of the paclitaxel molecule are substituted with a photocleavable moiety such as a chromophore. Typically, the chromophore is selected from the group comprising 2-nitrobenzyl ethers, carbamates or carbonates and their 4,5-dialkoxy substituted variants; 2-nitrophenylethyl ethers, carbamates or carbonates and their 4,5-dialkoxy substituted variants, or their p-substituted derivatives; oc-carboxy-2-nitrobenzyl ethers, carbamates or carbonates and their 4,5-dialkoxy substituted variants; 2(2-nitro- phenyl) ethyl ethers, carbamates or carbonates and their 4,5-dialkoxy substituted variants; coumarin-4-ylmethyl ethers, or carbonates and their 7-alkoxy, 6, 7-dialkoxy, 6-bromo-7-alkoxy or 7-dialkylamino substituted variants; p-hydroxyphenacyl ethers or carbamates and their meta-substituted derivatives or structurally related compounds. More specifically, the chromophore is 4, 5-dimethoxy-2- nitrobenyloxycarbonyl (Nvoc) or a structurally related compound. Further aspects of the invention relate to the use of these paclitaxel derivatives in biological, medical and pharmaceutical applications, in particular in cellbiology and cancer treatment. A closely related aspect is an antitumor medicament comprising the above paclitaxel derivatives.
EP2060572A1 Pyrazolopyridine derivative and phosphodiesterase (pde) inhibitor containing the same as active ingredient A novel pyrazolopyridine derivative is provided which is useful as a pharmaceutical drug having phosphodiesterase inhibitory activity. The pyrazolopyridine derivative is represented by the following general formula (1): [wherein R1 is a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms, or the like, R2 is an optionally substituted alkyl group having 1 to 6 carbon atoms or the like, R5 and R6 are independently a hydrogen atom or a halogen atom, R13 is a hydrogen atom or a halogen atom, n is 0 or 1, is a single or double bond, R3 is a hydrogen atom, a hydroxyl group, or the like, and R4 is a hydrogen atom, a phenyl group, or the like] or a pharmaceutically acceptable salt thereof, and a hydrate thereof.
WO2009148874A3 Gamma-lactam compounds for promoting bone growth The present invention provides compounds, compositions and methods for promoting bone growth. Compounds useful in the methods of the present invention include compounds of Formula 1, wherein each R1 and R2 is H, halogen, C1-6 alkyl, C1-6 alkoxy, C 1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkoxy, -OR4, -NR4R5, -SR4, -C(O)R4, -C(O)OR4, -C(O)NR4R5, -N(R4)C(O)R5, -N(R4)C(O)OR5, -N(R4JC(O)NR4R5, -OP(O)(OR4)2, -S(O)2OR4, -S(O)2NR4R5, -CN, cycloalkyl, heterocycloalkyl, aryl or heteroaryl. Each R4 and R5 is H or C1-6 alkyl. X is O, S or NR4. Y is an aryl ring system having 6-10 ring members or a heteroaryl ring system having 5-10 ring members where 1-3 ring members are each N, O or S. Subscript n is 1 or 2. The compounds also include salts, hydrates and isomers of the compounds of the present invention.
WO2013190569A3 Novel salts of sunitinib and preparation thereof Substituted aryl acrylic acid addition salts of Sunitinib (I), hydrate thereof, solvate thereof, processes thereof, and pharmaceutical composition thereof are provided. [Formula should be inserted here]
US20060194293 Rb1 gene induced protein (rb1cc1) and gene To provide a novel gene and protein involved in multidrug resistance in cancer, to elucidate functions of the gene and protein, to provide methods of detecting the gene and antibody against the protein and of testing and diagnosing cancer using the gene and antibody, we found a novel protein (RB1CC1) or polypeptide and gene thereof present in nucleus of human or animal cells and having transcription factor functions and/or functions inducing expression of retinoblastoma-1 gene (RB1 gene) or the gene product. We determined the amino acid sequence and cDNA sequence, conducted gene amplification and detection with primers hybridizing with the gene, tested for expression and mutation of the gene, discovered the gene relates to cancer cell proliferation and assayed cancers, prepared antibody against the protein and detected the protein using the antibody, whereby we found a relation between the protein and cancer cell proliferation, and assayed cancers.
CN101066280A Eye drop of deep sea water The eye drop of deep sea water features that it contains deep sea water to replace antibiotic and preservative. It has antiseptic and antiphlogistic effect, and functions of providing eye tissue with rich trace elements and nutritious components, remitting eye's fatigue and repairing eye's damage. It has no hidden hazard caused by antibiotic and preservative, no dependence and no toxic side effect.
CN101323616A Carbpenem derivates containing sulfhydryl thiazole The invention relates to a carbapenem derivative containing thyroidan as showed in a general formula (I), easily hydrolyzable ester thereof, a pharmaceutically acceptable nontoxic salt thereof, hydrate thereof and hydrate of the ester or salt thereof as well as a preparation method of the compound in the general formula (I). The invention also relates to medicine compositions containing the compounds and the application of the medicine compositions as active substances of medicines, in particular to the application of the compounds in preparing medicines for curing and/or preventing infectious diseases, wherein, the detailed definitions of each group refer to a specification.
EP2026825A2 Furanone-initiated polymers Polymers initiated with furanones and compositions containing such polymers are suitable for use in making textiles, medical devices, delivery agents, packaging materials, coatings for such items, and the like.
WO2012154077A1 Pharmaceutical composition for the treatment of tuberculosis and other infections, and method for producing said composition The invention relates to pharmacology, medicine, veterinary medicine and to the pharmaceutical industry, in particular to a method for producing original composite antimicrobial preparations for parenteral use, said preparations having increased therapeutic effectiveness in the treatment of severe forms of tuberculosis and other infectious inflammatory diseases. The proposed pharmaceutical composition comprises an antibiotic - aminoglycoside or capreomycin and highly dispersed nano-structured silicon dioxide as the active substance. The claimed method for the production of the pharmaceutical composition consists in mixing the antibiotic - aminoglycoside or capreomycin with the highly dispersed nano-structured silicon dioxide, characterized in that the mixture of the above-mentioned substances in ratios of 10:1 to 70:1 by weight, respectively, is subjected to mechanical processing by means of impact-abrading actions to increase the finely dispersed fraction weight portion. The mixture produced is used for preparing injection solutions.
CA2267947C Preparation of 3-fluoro oxindole derivatives The present invention relates to novel itermediates of formula (1) wherein the wavy bond (- -) represents the racemate, the (R)-enantiomer or the (S)-enantiomer; and R is hydrogen, a carboxyl-protecting group or a cation of an addition salt; or solvate thereof; and to the use thereof in a process for the preparation of certain 3-fluoro oxindole derivatives.
CN102512435A Application of 5,6,4'-trihydroxyl flavone-7-O-beta-D-glucuronide methyl ester and medicinal composition as well as preparation thereof The invention relates to the field of medicines, and discloses new application of 5,6,4'-trihydroxyl flavone-7-O-beta-D-glucuronide methyl ester to the field of pharmacy and a medicinal composition as well as a preparation thereof. The 5,6,4'-trihydroxyl flavone-7-O-beta-D-glucuronide methyl ester has the effects of improving sleep, such as prolonging sleep time, improving sleep incidence rate, shortening sleep latency and delaying aging, and can be used for preparing medicaments or health-care products for improving sleep and delaying aging.
WO2009063028A3 Substituted amides, manufacturing and use thereof as medicaments The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
WO2007065281A1 Quaternary 3 -amido, n-methylpyridinium salts as anti -inflammatory agents A novel group of anti-inflammatory compounds are salts composed of the anion of a nonsteroidal anti-inflammatory acid drug (NSAID) and the cation N(l)-methylnicotinamide, which both anion and cation moieties alone exhibit anti-inflammatory activity, and which in this combination have advantages over the individual compounds and in comparison to commercial anti-inflammatory products. The compounds are produced in analogy to processes known in the art. They are used for the preparation of new pharmaceutical formulations with anti-inflammatory and analgesic activity. The new pharmaceutical formulations exhibit several advantageous properties over preparations of prior art.
US20070287749 Bromfenac ophthalmic formulations and methods of use The present invention discloses a stability enhanced aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate. The present invention further discloses new bromfenac ophthalmic compositions which can potentially treat a broader patient population, and have greater stability properties, and may require a lower concentration or less doses of bromfenac then previously known bromfenac compositions. The present invention further comprises a method for treating inflammation and/or pain of the eye in a patient which method comprises topical application to the eye of a patient in need thereof of a therapeutically effective amount of a topical ophthalmic composition comprising bromfenac at a concentration of about 0.05% w/v to about 0.24% w/v.
US20110263679 C12orf48 as a target gene for cancer therapy and diagnosis Objective methods for diagnosing a predisposition to developing pancreatic cancer and prostate cancer, particularly pancreatic ductal adenocarcinoma (PDAC) and castration-resistant prostate cancer, are described herein. In one embodiment, the diagnostic method involves the step of determining an expression level of C12ORF48 using siRNAs targeting the C12ORF48 gene. The invention also features products such as siRNAs as well as to compositions containing them. The present invention further provides methods of screening for therapeutic agents useful in the treatment of C12ORF48 associated disease, such as a cancer, e.g. pancreatic cancer and prostate cancer, as well as methods of inhibiting the cell growth and treating or alleviating one or more disease symptoms. The invention also features products such as double stranded molecules, as well as vectors and compositions containing them.
CN101074228A Method for preparing medicine composition containing 1,3-oxathin cyclopentane nucleoside analogues PCT No. PCT/CA92/00321 Sec. 371 Date Feb. 1, 1994 Sec. 102(e) Date Feb. 1, 1994 PCT Filed Jul. 24, 1992 PCT Pub. No. WO93/03027 PCT Pub. Date Feb. 18, 1993The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one and pharmaceutically acceptable derivatives and pharmaceutical formulations thereof.
US20100266712 Prevention of Acute Kidney Injury The present invention provides a method of attenuating or preventing acute kidney injury occurring in a subject following cardiac surgery involving cardio-pulmonary bypass. The method comprises administration of at least one agent which cause alkalinization of urine to the subject at a level effective to cause alkalinization of the subject's urine. Preferably the agent which cause alkalinization of urine is selected from the group consisting of sodium bicarbonate, lactate, acetate, citrate, tromethamine and combinations thereof and is most preferably sodium bicarbonate.
CN102343015A Application of Tibetan medicament renqing mangiue to preparation of medicament for treating hepatocirrhosis The invention discloses novel application of Tibetan medicament renqing mangiue to preparation of a medicament for resisting hepatofibrosis. As proved by an animal experiment, renqing mangiue can be used for remarkably preventing the occurrence and development of rat hepatofibrosis induced by carbon tetrachloride (CCl4); renqing mangiue has a treatment effect on hepatofibrosis induced by dimethyl nitrosamine (DMN), and can be used for remarkably lowering the degree of hepatofibrosis; and the prevention and treatment effects of renqing mangiue are equivalent to those of a healthy energy strengthening and stasis dissolving capsule serving as a positive medicament.
WO2006108689A2 Process for preparing bicyclic compounds The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper, formulae (I) (Ia) wherein X is halogen; and the other substituents are as defined in the description.
WO2014026467A1 Bicyclic substituted pyrimidine compounds The present invention relates to the technical field of medicine and pharmacy, and particularly relates to bicyclic substituted pyrimidine compounds represented by general formula (I), pharmaceutically acceptable salts thereof or stereoisomers thereof, wherein R1, R2, R3, R4, R5 and R6 is as defined in the specification. The present invention also relates to preparation methods, pharmaceutical formulations, and pharmaceutical compositions of the compounds, and use of the compounds, pharmaceutical formulations and pharmaceutical compositions for preparing medicaments for treating and/or preventing sexual dysfunction diseases and diseases with lower urinary tract symptoms.
WO2005035477A1 Method of stabilizing compound having quinone skeleton and stabilized composition A method by which a compound having a quinone skeleton and coexistent with an antioxidant is stabilized; and a stabilized composition containing the compound having a quinone skeleton. The method of stabilizing a compound having a quinone skeleton in a composition comprising the compound having a quinone skeleton and an antioxidant is characterized by causing the compound and the antioxidant to coexist in an oily substance in such a state that at least either of the two is coated with an oil-insoluble coating medium or by causing the compound and the antioxidant to coexist in an aqueous substance in such a state that at least either of the two is coated with a water-insoluble coating medium. Thus, a compound having a quinone skeleton can be kept stable even when an antioxidant coexists with the compound having a quinone skeleton.
CN103446069A Oral solid composition of abiraterone and preparation method thereof The invention relates to an oral solid composition of abiraterone and a preparation method thereof. The composition contains abiraterone acetate with a particle size of 1-30 micrometers and pharmaceutic adjuvants.
CN101880310A Split heterocyclic 23-hydroxybetulinic acid derivatives and preparation method, preparation and application thereof The invention relates to the medicinal chemistry field, in particular to derivatives containing heterocyclic 23-hydroxybetulinic acid. The invention also discloses a preparation method of the derivatives, medicine compositions containing the compound and application of the compound on treating tumor diseases or symptoms.
EP1351680B8 Use of anethole-dithiolethione for preventing and treating drug-induced tendon toxicity The invention concerns the use of anethole-dithiolethione for producing a medicine for preventing drug-induced tendon toxicity.
CN103599230A Medicine for treating ulcerated chilblain The invention discloses a medicine for treating ulcerated chilblain. The medicine is characterized by comprising the following components: 3-7g of camphor, 2-8g of mint, 1-5g of resorcinol, 2-6g of boric acid, 1-5g of arnebia root oil, 3-7g of vitamin E, 2-8g of glycerin and 5-15g of honey. The medicine has the effect of obviously improving and relieving the signs and symptoms of the local extravasated blood and swelling and the ache of the ulcerated chilblain and has a unique curative effect; the curative ratio of the medicine reaches above 70%, and the total effective rate of the medicine reaches above 90%; the recurrence rate of the ulcerated chilblain is low.
WO2008077555A3 Substituted isoquinolines and their use as rho-kinase inhibitors The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
US7132435 Syn-1H-indazole-3-carboxylic acid (4-{[2-(2,3-dihydro-benzo[b]thiophen-6-yloxy)-5-fluoro-pyridine-3-carbonyl]amino}-cyclohexyl)-amide; useful as cyclic nucleotide phosphodiesterase-4 ( PDE-4 ) inhibitor This invention relates to nicotinamide derivatives of general formula (I): in which R1, X, Y, Z and R2 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.
US20080181854 antiinflammatory ascomycin derivative pimecrolimus in the form of a foam; inflammatory and hyperproliferative skin diseases and of cutaneous manifestations of immunologically-mediated diseases Pharmaceutical foam compositions substantially free of ethanol and comprising pimecrolimus in a carrier vehicle comprising a mixture of oily solvents amounting to at least 40% of the total weight of the composition and consisting of: i) hexylene glycol; ii) optionally oleyl alcohol; and iii) dimethylisosorbide and/or medium chain triglycerides; and additionally: iv) when oleyl alcohol is absent, water in an amount of less than 25%; v) at least one consistency agent; vi) at least one preservative; and vii) at least one surfactant/emulgator; and propellant gas for foaming; and optionally further conventional excipients. They are indicated for use in the treatment of various skin, nail and mucosal diseases.
US20110046229 Controlled Release Drug Delivery Systems And Pharmaceutical Compositions Formed Therewith The present invention relates to controlled release drug delivery systems. In one embodiment, the present invention relates to controlled release drug delivery systems comprising a combination of at least one polyacrylic acid and at least one enteric polymer. In another embodiment, the present invention relates to a controlled release pharmaceutical composition comprising the combination of at least one active pharmaceutical ingredient and a controlled release drug delivery system, where the controlled release drug delivery system comprises the combination of at least one polyacrylic acid and at least one enteric polymer.
CN101816659A Anti-tumor medicament The invention discloses an anti-tumor medicament, and belongs to the technical field of the pharmaceutical chemical industry. The anti-tumor medicament is 6-substituted-5,6-dihydro pyrrolo[3,4-d]pyridine-7-ketone(IV) with a structural general formula shown in the specifications. The medicament is a composition with high activity for suppressing protein kinase, has easy preparation method, convenient source of raw materials and easy realization of industrialization, and meets the requirements of the preparation of the medicament for clinical cancer therapy.
WO2013157555A1 Novel aplysiatoxin derivative and anticancer agent containing same The invention provides an aplysiatoxin derivative represented by formula (I), or a pharmaceutically acceptable salt thereof, that is a PKC activator having no carcinogenesis-promoting activity that can serve as an alternative to Bryo-1 as a novel compound that can be used as an anticancer agent. (In formula (I), R1 is a hydrogen atom or hydroxyl group; R2 is a hydrogen atom or methyl group; R3 is a hydrogen atom or methyl group; R4 is a hydrogen atom or methyl group; R5 is a hydrogen atom or methyl group; and R6 is represented by a substituent selected from any of a hydrogen atom, halogen atom, acetylamino group, hydroxyl group, or optionally substituted alkyl group having 1-5 carbon atoms.)
CN102743458A Formula of health drug with effects blood fat regulating and immunity increasing The invention provides a formula of a health drug with effects blood fat regulating and immunity increasing, and relates to a health drug. The formula comprises: 7-20 g of a broccoli extract, 3.5-8 g of red kojic rice, 5-9 g of a hawthorn extract, 5-12 g of a ginkgo extract, 3.5-6 g of a salvia miltiorrhiza extract, 3.5-7 g of allitricin, 1.5-3 g of rhubarb, 1.5-5 g of safflower, and 3.5-10 g of microcrystalline cellulose. The preparation process comprises: respectively crushing the red kojic rice, the salvia miltiorrhiza, the rhubarb and the safflower, and screening with an 80-100 mesh sieve; respectively taking the resulting powders, and weighing the resulting powders, the broccoli extract, the hawthorn extract, the ginkgo extract, the allitricin and the microcrystalline cellulose according to a certain ratio; mixing the weighed raw materials for 45 minutes (it is ensured that a uniform mixing treatment is performed); then filling the mixture into capsules (the filled materials are controlled according to an internal control standard); and carrying out screening, polishing, inner packaging, outer packaging, testing and warehousing. The health drug of the present invention has characteristics of immunity enhancing, blood fat regulating, human immunity increasing, hyperlipemia patient life quality improving, no side effect, and no adverse reaction. In addition, according to the present invention, the modern preparation technology is adopted, and the advanced quality control method is adopted, such that the product has characteristics of safety, stability, and controllable quality.
WO2013076178A1 Crystalline salts of r)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1h-imidazol-4-yl)-propionic acid The invention relates to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1 -cyclohexyl- 1 H-imidazol-4-yl)-propionic acid which is in a crystalline form or in at least partially crystalline form as a monohydrate or anhydrate, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor).
US20110300113 Death Receptor CD95 Controls Neurogenesis of Adult Neural Stem Cells in Vivo and in Vitro The present invention relates to the activation of the CD95L/CD95 system for inducing neuronal differentiation in vitro and in vivo and the use of CD95L compositions to effect differentiation.
CN101693032A Composition for treating feline infectious anaemia and method for preparing the composition The invention discloses a composition for treating feline infectious anaemia and a method for preparing the composition, and aims at providing a composition for treating feline infectious anaemia with rapid effect, safe use, efficiency and high performance and a method for preparing the composition. The composition is composed of the following components according to the weight percentage: doxycycline hydrochloride 2 to 10%, algocalmin 2 to 15%, taurine 2 to 10%, metoclopramide HCL 0.1 to 0.8%, and the allowance is anhydrous dextrose. The composition for treating feline infectious anaemia and the method for preparing the composition adopt the Doxycycline Hydrochloride to kill pathogeny, and control secondary invader and rickettsial infection, algocalmin has the antipyretic and anti-inflammatory functions, taurine has the antipyretic and hepatoprotective functions, the Metoclopramide HCL has the functions of prompting gastrointestinal peristalsis and prompting ingestion, and treatment of feline infectious anaemia through combination and matching of the drugs has rapid effect and prominent curative effect, and can effectively reduce the pain of cats, and reduce trouble and obsession of culturists.
US20090182034 containing preponderance of cis doxepin isomer over trans doxepin isomer; decreased sedative effects; conjunctivitis Therapeutic compositions of doxepin and having a preponderance of the cis doxepin isomer over the trans doxepin isomer provide therapeutic effects for affective, painful, or allergic disorders without the sedative effects commonly experienced with compositions having a preponderance of the trans doxepin isomer.
WO2014082354A1 Crystal form of chidamide, preparation method and use thereof The present invention belongs to the field of pharmaceutical chemistry, and disclosed are two crystal forms of Chidamide, that is, Chidamide crystal form A and Chidamide crystal form B, and the method for preparing the new crystal forms of Chidamide. The Chidamide crystal form A and Chidamide crystal form B of the present invention can be used for preparing drugs for treating diseases related to cell differentiation and proliferation.
WO2013186159A1 New diazaspirocycloalkane and azaspirocycloalkane The invention provides novel compounds having the general formula (I), wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.
US20070185007 Inhibition of HiV integrase compounds Aza-quinolinol phosphonate compounds and methods for inhibition of HIV-integrase are disclosed. Formula (I). Ar is aryl or heteroaryl connecting R6 to L. L is a bond or a linker connecting a ring atom of Ar to N. The ring atoms, X1-X5 may be N, substituted nitrogen, or substituted carbon, and form rings. The compounds include at least one phosphonate group covalently attached at any site.
WO2006099685A1 Method for the prophylaxis or treatment of carcinomas There are described methods for the prophylaxis or treatment of carcinomas in a mammalian subject comprising administering a metal complex having anti-inflammatory activity to the mammal. Typically, the complex is a complex of at least one metal and at least one non-steroidal anti-inflammatory drug (NSAID). Suitable complexes include a complex of a metal and a carboxylate, or a derivative of a carboxylate, having anti-inflammatory activity.
CN101890044A External medicament for treating infant ulcerative stomatitis The invention discloses an external medicament for treating infant ulcerative stomatitis. The external medicament is characterized by comprising the following materials in percentage by weight: 1.85 to 1.95 percent of iodine, 1.85 to 1.95 percent of potassium iodide, 0.9 to 1.0 percent of tetracaine and 95.1 to 95.3 percent of glycerol. The external medicament has the advantages of simple materials, convenient operation, low side effect and high cure rate, and is particularly suitable for treating the infant ulcerative stomatitis.
WO2011006097A3 Methods For Treating Toxicity Provided herein are, inter alia, methods and compositions for treating acetaminophen toxicity.
WO2014091239A1 Novel pharmaceutical formulations and their use in the treatment of periodontal disease The present invention relates to novel treatments of periodontal disease by administering a suitable formulation of a cyclophilin inhibitor. The present invention further relates to novel pharmaceutical compositions containing said cyclophilin inhibitor compounds.
WO2009132228A1 Chitosan-containing protective composition Body tissue and structures may be protected using a fluid containing a mixture of partially crosslinked polysaccharide and a further crosslinker. The mixture desirably is sprayable, forms a fluid protective layer via in situ crosslinking, desirably does not drip or run from a treatment site, and may avoid the use of more rapidly curing but potentially less bioacceptable crosslinkers at the treatment site.
US20120207839 Mineralized Collagen/Bioceramic Composite and Manufacturing Method Thereof The present invention discloses a mineralized collagen/bioceramic composite useful as a hard tissue replacement material or substitute material, comprising about 10% to 95% by weight of mineralized collagen and about 5% to 90% by weight of bioceramics, and a method of manufacturing the same. Wherein, the mineralized collagen is used as a binder for the bioceramics, such as calcium phosphate ceramics, calcium sulfate ceramics, calcium carbonate ceramics, and other biocompatible ceramics. The bioceramic used in the mineralized collagen/bioceramic composite can be either in powder form or in granular form.
US20110152305 Films and particles Described herein are compounds and processes that can be used to prepare polymer-based films, particles, gels and related compositions, and processes for delivery of agents, and other uses.
US20110104306 Novel compositions and methods for the identification, assessment, prevention and therapy of human cancers The present invention is directed to the identification of markers that can be used to determine whether tumors are sensitive or resistant to a therapeutic agent. The present invention is also directed to the identification of therapeutic targets. The invention features a number of “sensitivity markers.” These are markers that are expressed in most or all cell lines that are sensitive to treatment with an agent and which are not expressed (or are expressed at a rather low level) in cells that are resistant to treatment with that agent. The invention also features a number of “resistance markers.” These are markers that are expressed in most or all cell lines that are resistant to treatment with an agent and which are not expressed (or are expressed at a rather low level) in cells that are sensitive to treatment with that agent. The invention also features marker sets that can predict patients that are likely to respond or not to respond to an agent.
US20110224302 Difluorophenyldiacylhydrazide derivatives Novel difluorophenyldiacylhydrazide derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and complaints such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in any type of fibroses, inflammatory processes, tumours and tumour diseases
WO2010120996A1 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses A compound of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
WO2012001418A1 Multi-metallic complexes The invention provides complexes comprising two octahedrally coordinated metal centres having the same absolute configuration and which are linked by a plurality of linkers whereby to form a flexible helical structure. Preferred complexes are those shown schematically by way of the following structure: formula (I) (wherein each M independently denotes a transition metal ion; each A'—A independently denotes a bidentate unit; each A' and A independently denotes a donor atom within said bidentate unit; and each L independently denotes a linker). The complexes find use in a wide range of medical applications, for example as antimicrobial agents and in treating cancer. Other uses include the delivery of biomolecules such as nucleic acids in methods of gene therapy.
US20140099279 Metal alloys for medical devices A medical device that is at least partially formed of a novel metal alloy, which novel metal alloy improves the physical properties of the medical device.
WO2011072292A2 Phase changing formulations of rna and rna derivatives The present invention is based, at least in part, upon discovery of a process for identifying phase changing peptides. Such phase changing peptides are capable of enhancing in vitro and in vivo delivery of oligonucleotides (e.g., dsRNAs) in lipidic, vesicular, micellar and/or naked oligonucleotide formulations.
EP2786998A1 Thienyl [3, 2-d]pyrimidin-4-one compounds, preparation method, pharmaceutical compositions and use thereof Disclosed are new thienyl [3, 2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.
US7615564 Such as N5-[1-(2-chlorobenzyl)tetrahydro-1H-3-pyrrolyl]-5-isoquinolylamine; Rho kinase inhibitors; hypertension, asthma, angina pectoris, cerebrovascular contraction, peripheral circulatory disorder, threatened premature birth, glaucoma, vision disorders, autoimmune diseases, chronic renal failure An objective of the present invention is to provide compounds having Rho kinase inhibitory activity and useful for the treatment of diseases mediated by Rho kinase. The compounds according to the present invention are those represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein Q represents phenyl, pyridyl, pyrrolyl, thienyl, or furyl; these groups are optionally substituted by one or two halogens or alkyl, nitro, or amino groups; and p is 2 or 3.
US20130065949 Microrna mirna-31 as a therapeutic approach for the treatment of cancer The present invention generally concerns methods and compositions for treating and/or preventing cancer with microRNAs. In specific embodiments, the present invention encompasses a particular microRNA, microRNA-31, as useful in cancer therapy and/or prevention. Specific cancers may be treated, including at least ovarian, prostate, urothelial, osteosarcoma, and glioblastoma.
EP2157085A1 Oxazole, derivatives of tetracyclines This invention provides compounds of the formula: wherein A", X and Y are defined in the specification. These compounds are useful as antibacterial agents or may be hydrolysed to give 9-(2-substituted aminomethylcarbonylamino)substituted-6-demethyl-6-deoxytetracycline derivatives.
US8337816 Comprising inhalable medicament particles having a mass median aerodynamic diameter no greater than 10 mu m and 50% of a non-respirable excipient fraction comprising low density excipient particles having an aerodynamic diameter greater than 10 mu m and a geometric diameter greater than 30 mu m A dry powder pharmaceutical composition comprising (i) a medicament particle fraction comprising medicament particles with an aerodynamic diameter no greater than 10 μm; and (ii) at least 50% of a non-respirable excipient fraction comprising low density excipient particles with an aerodynamic diameter greater than 10 μm and a geometric diameter greater than 30 μm. In additional embodiments of the invention, the pharmaceutical composition includes a respirable excipient fraction comprising excipient particles with an aerodynamic diameter no greater than 10 μm. In a preferred embodiment of the invention, the non-respirable excipient particles include pores adapted to receive a portion of the respirable excipient fraction and/or the medicament fraction.
CN101744903A Dropping liquid for treating otitis media and preparation method thereof The invention relates to a medicament for treating otitis, in particular to a dropping liquid for treating otitis media. The dropping liquid is prepared from golden thread, borneol and purified water according to the formula amount by the following steps: heating and decocting golden thread which is cut into pieces in the container; after the decoction is boiled, boiling the decoction for a preset time with low heat; adding the formula amount of borneol to boil for a preset time; turning off the fire and removing dregs; adjusting the medical solution; and sterilizing the adjusted medical solution and filling the sterilized medical solution into finished products. By adoption of the novel formula and provement of the clinical test, the invention has quick response to the adaptation disease and short treatment period, and addresses both the symptoms and root causes on diminishing inflammation and relieving pain. When the test is carried out on the tenth day, 98 patients in 100 tested patients have been healed, only two tested patients are still not healed, thus, the dropping liquid has relapse prevention after healing, particularly has more ideal curative effect on the suppurative chronic otitis media, not only eliminates pain for the patient, but also obviously reduce the treatment cost, has no toxic or side effects and easy preparation, and is the treatment medicament preferred by each medical institution.
US20100063085 Method of treating learning impairment in down's syndrome subjects The present invention provides compounds for use in the preparation of pharmaceutical formulations and medicaments, which alleviate learning and/or mental impairment in people suffering from Down's syndrome.
CN102807569A Compound with clam and hypnosis functions, and preparation method and application thereof The invention discloses a compound expressed in a formula 1. The structural formula of the compound is as follows, wherein R is alkyl group with H and C1-10, -COOR1, -CH2-C6H4-R2, the R1 is alkyl group with the H or the C1-10, the R2 is H, halogen, nitro or alkyl group with C1-5, and R3 is alkyl group with C1-5, arene group of C6-12 or substitutional alkyl group of C1-5. The invention also provides the application of the compound. The compound disclosed by the invention can obviously inhibit spontaneous movement times of a mouse, and the compound has a significance difference or an extreme significance difference by comparing each time point and a negative contrast group, so that the compound can be used as a medical active ingredient of a medicine preventing insomnia and further can be used for developing new medicines which are relatively good in medical effect and relatively small in untoward effect, thus having obvious social benefits and economic benefits. The method provided by the invention has the advantages that the method process line is very simple, the cost is relatively low, the yield of products is relatively high, and the requirements on industrial and large-scale production can be met.
EP1586642A2 Tumor supressor genes, proteins encoded thereby and use of said genes and proteins The present invention is based on the pioneering finding that inhibition of expression of certain genes counteracts the cytokine-induced cell death. As long as these genes function normally, cytokine induces cell death; once the expression of said genes is inhibited, the cytokine-induced cell death is inhibited. Its follows therefrom that the normal expression is cytokine-induced cell death. In HeLa cells IFN-gamma induces a biphasic process, which comprises an initial cytostatic phase and a subsequent cytotoxic phase (programmed cell death). The novels genes discovered in accordance with the present invention were found to affect only the later, cytotoxic phase. These genes, referred to as "DAP" (death-associated protein) genes, include DNA molecules which comprise a coding sequence encoding the expression products of the DAP genes or expression products having a similar biological activity.
CN1969872A Method for preparing colon targeted pill of lincomycin used for poultry and livestock The invention relates to Lincomycin colon-targeting pills which comprise Lincomycin as the main ingredient, and blank pellets are employed. The medicinal layer comprises Lincomycin, 8% retarding layer of hexadecyl alcohol, 2% retarding layer of HPMC, 15% pH responsive film of acrylic resin S100. The prepared colon-targeting pills are of retarding-and-pH responsive combined type which can achieve the positioned medicinal release on the animal's colons, the curative effects for localized infection and general infection can be improved substantially.
US7160871 Nitrate esters of corticoid compounds and pharmaceutical applications thereof Compounds of the formula and use of the compounds as medicaments.
CN103263498A Application of Chaenomeles speciosa (sweet) Nakai extract in pharmacy The invention relates to novel application of a Chaenomeles speciosa (sweet) Nakai extract, specifically to application of oleanolic acid, ursolic acid, oleanolic saponins and ursolic saponins in the extract in the pharmaceutical field. The extract has effects on inhibition of DNP-BSA induced RBL-2H3 mast cell degranulation, DNP-BSA induced mBMMCs mast cell degranulation, calcium ionophore A23187 induced RBL-2H3 mast cell degranulation and Thapsigargin induced RBL-2H3 mast cell degranulation and on xylene-induced acute inflammation like ear swelling of mice and has a high medicinal value.
US20080039419 Integrin-linked kinase and its uses ILK genetic sequences and methods of use are provided.
EP1343860B1 A process for preparing vegetable oil fractions rich in non-tocolic, high-melting, unsaponifiable matter A vegtable oil fraction rich in non-tocolic, high-melting, unsaponifiable matter is prepared by the following steps: A vegetable oil having a slip melting point of not more thatn 30°C and a content of unsaponifiable matter of at least 0.5% by weight is hydrongenated to fully saturate the fatty acids of the glycerides and to reach a slip melting point of at least 57°C. To the hydrongenated oil is added from 1 to 75% by weight of the unhydrogenated starting oil or another oil having a slip melting poing of not more than 30°C in order to act as a carrier and vehicle for the unsaponifiable matter. Then, a solvent is added to the oil mixture in a ratio between oil and solvent from 1:2 to 1:20, and the mixture is heated to transparency. The oil/-solvent-mixture is cooled in one or more steps to a final temperature in the range from -35 to+30°C, and the precipitated high-melting fraction(s) is (are) filtered off. The filtrate is desolventised, leaving a fraction rich in unsaponifiable matter. By this process very high concentrations of in particular the non-tocolic, higher melting unsaponifiables can be achieved, and the composition of the glyceridic part of the enriched fraction can betailored to specific applications. Also, a novel blood cholesterol-lowering effect of the unsaponifiable constituents from shea butter has been found.
WO2005023241A1 The use of fumaric acid derivatives for treating cardiac insufficiency, and asthma According to a first aspect the invention relates to the use of fumaric acid derivatives selected from the group consisting of dialkyl fumarates, monoalkyl hydrogen fumarates, fumaric acid monoalkyl ester salts, fumaric acid monoamides, monoamido fumaric acid salts, fumaric acid diamides, monoalkyl monoamido fumarates, carbocyclic and oxacarbocyclic oligomers of these compounds and mixtures thereof for preparing a drug for the treatment or prevention of cardiac insufficiency, in particular left ventricular insufficiency, myocardial infarction and angina pectoris. According to a second aspect the invention relates to the use of fumaric acid derivatives, selected from the group consisting of dialkyl fumarates, monoalkyl hydrogen fumarates, fumaric acid monoaklyl ester salts, fumaric acid monoamido fumaric acid salts, fumaric acid diamides, monoalkyl monoamido fumarates, carbocyclic and oxacarbocyclic oligomers of these compounds and mixtures thereof for preparing a drug for the treatment of asthma and chronic obstructive pulmonary diseases, especially asthma caused by allergies, infections, analgesics, job conditions or physical effort, mixed forms of asthma, or asthma cardiale.
US7183075 Purified and isolated potassium-chloride cotransporter nucleic acids and polypeptides and therapeutic and screening methods using same KCC2, KCC3 and KCC4 potassium-chloride cotransporter proteins, and nucleic acid molecules encoding the same. Recombinant host cells, recombinant nucleic acids and recombinant proteins are also disclosed, along with methods of producing each. Isolated and purified antibodies to KCC2, KCC3 and KCC4 homologs, and methods of producing the same, are also disclosed. KCC2, KCC3 and KCC4 gene products have biological activity in potassium-chloride cotransport. Thus, therapeutic methods involving this activity are also disclosed.
CN101954069A Anticancer application of recombinant human manganese superoxide dismutase The invention discloses anticancer application of recombinant human manganese superoxide dismutase. The invention also discloses a medicinal composition containing the recombinant human manganese superoxide dismutase and adriamycin, which has a good anticancer effect. The medicament composition of the invention has no toxic or side effects and has a promising medicinal prospect.
US20120088784 Substituted Aromatic Compounds and Pharmaceutical Uses thereof The present invention relates to substituted aromatic compounds of Formula I and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention or treatment of (i) blood disorders, (ii) renal disorders, a nephropathies, or renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders.
CN101422478A Etoposide slow-release drop-pills and preparation method thereof The invention relates to the technical field of medicine and relates to an etoposide sustained release dripping pill which has the advantages of small use dosage, durable and stable drug effects, high bioavailability, low cost and convenient industrialization and large production. The technical proposal is as follows: the weight percentage of the etoposide or the pharmaceutically acceptable salt thereof in the etoposide sustained release dripping pill is 10 to 35 percent; 20 to 43 percent of water-insoluble substrate and 30 to 53 percent of water-soluble substrate are used as the substrates; the water-insoluble substrate is selected from stearic acid and octodecyl alcohol; and the water-soluble substrate is selected from poloxamer and polyoxyethylene (40) stearate. The preparation technique is as follows: after the substrates are heated and molten, the etoposide or the pharmaceutically acceptable salt thereof is added to prepare a suspension liquid; the suspension liquid is put into a dripping tank, the insulation can of which is provided with a water dropper, dripped into a condensate liquid, condensed into spherical shape and sucked, thus obtaining the product. The condensate liquid is simethicone or liquid olefin, and the simethicone is preferred. The heating-melting temperature is between 80 and 100 DEG C; and the temperature for the suspension liquid to be dripped into the condensation liquid is controlled between 80 and 110 DEG C.
EP1311504B1 Tetrazolyl-phenyl acetamide glucokinase activators Tetrazotyl-phenyl acetamides of formula (1) wherein Z is (2) one of R1 or R2 is (3) and the other is hydrogen, halogen, lower alkyl sulfonyl, perfluoro lower alkyl, cyano, or nitro; R3 is cycloalkyl; R4 is -C(O)-NHR6 or a five- or six-membered heteroaromatic ring connected by a ring carbon atom to the amide group, are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.
CN103751090A Metronidazole-containing external drug The invention provides a metronidazole-containing external drug. The metronidazole-containing external drug utilizes metronidazole as a medicinal active component. The metronidazole-containing external drug contains a medicinal matrix for external use. The metronidazole-containing external drug can be prepared simply, can be processed to form external preparations such as a liniment and gelata, and has the advantages of uniform active component dispersion, simple preparation processes, mild drug properties, clinical use convenience, high patient compliance and reliable treatment effects.
CA2630595A1 Foam wafer containing a polyvinyl alcohol-polyethyleneglycol-graft copolymer The invention relates to a flat administration form, which is soluble or disintegrates in an aqueous medium, for releasing at least one active substance into a body opening or body cavity, comprising a polymer-matrix which is in the form of a solid foam comprising a chamber or cavities, in addition to at least one pharmaceutical or cosmetic active substance. Said administration form is characterised in that the polymer of the matrix is a polyvinyl alcohol-polyethyleneglycol-graft polymer. The invention also relates to a method for producing said type of administration forms.
WO2006094034A1 Cinnoline compounds and their use as liver x receptor modilators This invention relates to cinnoline-based modulators of Liver X receptors (LXRs) of formula (I) wherein R2 is a ring containing residue, particularly a phenyl residue. These compounds are useful in the treatment of cardiovascular diseases.
US20090048330 Compound from Antrodia camphorata and the use thereof The present invention relates to novel compounds from Antrodia camphorata and the use thereof.
EP1165106B1 Composition and method for inducing apoptosis in prostate cancer cells by m-dna and mcc A method for treating prostate cancer in an animal, wherein a composition comprising Mycobacterium phlei (M. phlei) DNA (M-DNA) and M-DNA preserved and complexed on M. phlei cell wall (MCC) is administered to the animal in need of such treatment in an amount effective to have an anti-neoplastic effect on cancer cells in the prostate of the animal.
WO2007073297A1 Pyrazoles for the treatment of gerd and ibs The present invention relates to novel pyrazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS) . The compounds are represented by the general formula (I) wherein R1, R2, R3 and Y are as defined in the description. For example, R1 may be hydrogen or alkyl, R2 may be hydrogen or alkyl, R3 may be alkoxy and Y may be a carbonylamino linked substituent containing an aryl group.
CN1827634A Nitrate derivatives of glycyrrhetic acid and glycyrrhetinic acid and pharmaceutical use thereof Disclosed are nitrate derivant of glycyrrhizic acid or glycor represented by formula Ia and Ib and its nontoxic salt which can be accepted in the sphere of pharmacy, their precoss for preparing, and components and usage of the drugs which contain these compounds.Thereinto, R1, R2 and R3 stand for hydroxyl or -X-L-oxo-oxonitryl (X stands for oxygen,imino; L stands for alkyl with 2-6 of canbon atoms, substituted alkyl or cycloalkyl, hydroxyl amino acid residue or N,Ní»-disubstituted piperazine); R3 stands for hydrogen, oxonitryl or carbonyl -Lí»oxo-oxonitryl (Lí»stands for alkyl with 1-6 of canbon atoms, substituted alkyl or cycloalkyl, aralkyl, N,Ní»-disubstituted piperazine); in formula Ib, R1, R2 and R3 may be the same or different, but in which at least one of them contains -X-L-oxo-oxonitryl; in formula Ib, at least one of R3 or R4 must contain oxonitryl. In formula Ia and Ib, hydrogen of 18-carbon can be alpha-isomer or beta-isomer.
CN103054897A Borneol fluorine rapid-healing scaling liquid The invention relates to a medicine for treating scale, and in particular relates to a borneol fluorine rapid-healing scaling liquid which is prepared from the following materials by weight: 2-3g of borneol, 2.5-3g of dried alum, 2-3g of norfloxacin, and 480-520g of normal saline of 0.9%. In the prescription, the borneol has the functions of clearing away heat and toxic materials, cooling blood, preventing corrosion and relieving itching, diminishing swelling and relieving pain; the dried alum has the functions of antibiosis, sore healing, muscle regeneration and scab prompting; the norfloxacin has the functions of inflammation diminishing and antibiosis; and the normal saline of 0.9% has the functions of cleaning and antibiosis and can be used as a lyase solvent and a preservative; the borneol fluorine rapid-healing scaling liquid combines the four medicines, the prescription is rigorous and scientific, and the curative effect is definite, so that the borneol fluorine rapid-healing scaling liquid is applicable to I-grade, II-grade and partial III-grade scale, and is short in treatment course, rapid to heal and remarkable in curative effect when being compared with similar medicines for treating scale.
CN2843449Y Externally-applied plaster for treating acute sprain and contuse The utility model discloses an externally-applied plaster for treating acute sprain and contuse, which is composed of a mounting layer, a hydrophilic gel layer and a protecting film layer, wherein the mounting layer comprises a sealing layer, an isolating layer, a pressure-sensitive adhesive layer from the inner part to the outer part in sequence; the sealing layer is provided with a separating device which can be removed, and the separating device divides the sealing layer into two separate cavity bodies; the two cavity bodies are respectively filled with chemical refrigerant. The utility model makes skin achieve the effect of refrigeration and comfort for a long time through the hydrophilic gel layer and controls the temperature and the time of freezing through the control to the weight of ammonium nitrate of the chemical refrigerant, sodium carbonate decahydrate and water. Thus, the utility model avoids the consequences of the inconvenient use, large degree of casualness and easy generation of non-freezing frostbite brought by refrigeration therapy, and the utility model is particularly suitable to be used for first aid of athletes in an athletic field.
US20080125416 Sigma Receptor Inhibitors The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
US20100297220 Pharmaceutical Formulation And Method For Treating Acid-Caused Gastrointestinal Disorders Pharmaceutical formulations in the form of a powder for suspension comprising at least one proton pump inhibitor in micronized form; at least one antacid; and at lest one suspending agents are provided herein. Also provided herein are methods for making and using pharmaceutical formulations comprising at least one proton pump inhibitor and at least one antacid.
CN103690519A Application of salvianolic acid A in preparation of medicine for treating tumour multi-drug resistance The invention relates to the field of natural medicines, and discloses application of salvianolic acid A in preparation of a medicine for treating tumour multi-drug resistance. Compared with salvia extracts of tanshinones, the salvianolic acid A disclosed by the invention has good water solubility, and therefore, the salvianolic acid A has better bioavailability. According to the invention, the salvianolic acid A has obvious inhibiting effect to drug-resistant tumour cells; the mechanism is as follows: apoptosis of drug-resistant tumour cells is induced through up regulation of expression of proapoprotic protein is up-regulated and down regulation of expression of inhibitor of apoptosis protein; tumour drug-resistant protein P-gp expression is inhibited by increasing active oxygen expression level of drug-resistant tumour cells, so that tumour multi-drug drug-resistant cells are overcome, and therefore, the salvianolic acid A disclosed by the invention has the application prospect for preparing the medicine for overcoming tumour multi-drug resistance.
CN103127092A Application of Aphanamixoid A to medicine for treating osteoporosis caused by antiestrogen insufficiency The invention discloses novel application of Aphanamixoid A to prevention and treatment of osteoporosis. The osteoporosis is one of key diseases endangering human health, with aging of population, the number of patients suffering from the osteoporosis is gradually increased, and the situation brings huge social, medical and economic burden to the whole world. Effective medicine for treating the disease is still absent even though domestic and foreign relevant experts and scholars pay great attention to prevention and treatment of the disease. In-vivo tests show that the Aphanamixoid A has significant anti-osteoporosis functions. Test results show that the Aphanamixoid A can inhibit bone conversion percent improvement caused by ovariectomization, reduce bone destruction, improve blood calcium concentration and be beneficial for bone deposition. The Aphanamixoid A has the function of treating the osteoporosis caused by antiestrogen insufficiency and is free of estrogen-like side effects.
US8012996 Methods and composition for inhibition of angiogenesis The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as EM-12 and its derivatives have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.
US6869621 Diet composition comprising raw foods and dietary fibers The present invention relates to a diet composition comprising brown rice, job's tear, red beans, buckwheat, Italian millet, Indian millet, white beans, black beans, black rice, barley, brown rice sprouts, kale, matured pumpkin (Curcurbia moschata), carrot, Angelica, cabbage, wild Lanceolate root, Lotus root, radish, green radish, mugwort, pine needles, laver, sea mustard, sea tagle, Shiitake mushroom, Reishi mushroom, soy peptide, isolated soy protein, L-carnitine, Hibiscus extract, green tea extract and solomon's seal extract. The composition is useful in reducing body weight and body fat; controlling body shape; and lowering serum cholesterol and neutral fat.
US20110212154 Biodegradable Implantable Drug Delivery Device The invention relates to biodegradable and implantable devices for the in situ delivery of a pharmaceutical composition to a human or animal that comprise a generally discoid body, having at least one aperture through which the body is anchorable by suture, and that are formed from biodegradable polymeric compositions. The invention relates to methods of manufacturing devices for the in situ delivery of a pharmaceutical composition to a human or animal that comprise a generally discoid body, having at least one aperture through which the body is anchorable by suture, and that are formed from biodegradable polymeric compositions. The invention relates to a therapeutic method that comprises inserting a biodegradable and implantable device that comprises a generally discoid body, having at least one aperture through which the body is anchorable by suture, and that is formed from a biodegradable polymeric composition, into a body cavity of a human or animal.
US20070155654 Novel formulations Stable, soluble insulin formulations having both a fast and a long action.
WO2014144654A1 Compounds for stabilizing ryanodine receptors from aberrant levels of calcium release Disclosed herein are methods and compositions comprising compounds capable of normalizing neuronal calcium dyshomeostasis. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, Pick's disease, chronic traumatic encepholopathy, traumatic brain injury, stroke, cerebellar ataxia, multiple sclerosis, Down syndrome, and aging-related CNS disorders.
CN101411688A Compound lincomycin hydrochloride soluble powder for bird and preparation method thereof The invention relates to compound lincomycin hydrochloride soluble powder for poultry, which is characterized in that the powder is prepared by the even mixing of the following components in weight portion: 10 to 25 portions of lincomycin hydrochloride, 5 to 20 portions of tylosin phosphate, 5 to 15 portions of sulfadiazine sodium, and 40 to 80 portions of glucose. A preparation method comprises the following steps: (1) weighing 10 to 25 portions of the lincomycin hydrochloride and 10 to 30 portions of the glucose according to the weight portion, and stirring and mixing the lincomycin hydrochloride and the glucose for 10 to 25 minutes; (2) putting 5 to 20 portions of the tylosin phosphate and 5 to 15 portions of the sulfadiazine sodium into the lincomycin hydrochloride composition for stirring and mixing 10 to 25 minutes; and (3) after combining the compositions prepared in steps (1) and (2), adding the rest of the glucose into the compositions for stirring 15 to 20 minutes and mixing evenly. The compound lincomycin hydrochloride soluble powder has the advantages of reasonable composition, simple preparation, remarkable curative effect, and special effect for treating enterotoxemia syndrome proved by clinical application by adopting the compound preparation.
US20120035249 Targeted Mucosal Treatment of Obesity and Diabetes A technique for treating obesity, diabetes, and other endocrinological disorders by removal of the omentum by endoscopic and oral approaches is described herein. The removal of the omentum interferes with the glucose absorption or ghrelin production thereby improving and correcting the obesity and diabetes.
WO2005044275A1 Use The present invention relates to the use of roscovitine, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for treating multiple myeloma.
CA2272063C Antithrombotic organic nitrates Compounds, or their compositions, of the general formula: A-(X1-NO2)to or their salts, for the preparation of medicaments for antithrombotic application, where: to is an integer equal to I or 2; X, is an alkylene connecting bridge, A is the residue of cardiovascular products, preferably timolol or enalapril.
WO2012118172A1 Drug for improving central functions during pain Provided is a drug for improving central functions during pain having as active ingredients a narcotic analgesic and a compound having an inhibitory effect on GIRK channel activation current (a GIRK channel inhibiting compound). This drug for improving central functions during pain comprises a GIRK channel inhibiting compound such as tipepidine and a narcotic analgesic such as morphine, wherein the dosis of the GIRK channel inhibiting compound does not by itself exhibit an analgesic effect on pain, nor does the dosis of the narcotic analgesic by itself exhibit an analgesic effect on pain, but this drug improves central functions during pain with few side effects when the doses of the two components are combined.
CN102145180A Application of miR-34c in preparation of medicaments or health-care products for treating or preventing liver cancers The invention discloses application of non-coded small RNA gene miR-34c in diagnosis and treatment of primary liver cancers. The miR-34c can effectively inhibit hepatitis B virus (HBV) related liver cancers. Discovered by researches, the miR-34c has remarkable low expression in HBV transgenic mice liver cancer tissues and HBV infected liver cancer cell strains; and after expression vectors of the miR-34c are transfected to liver cancer cells HepG2.2.15, the miR-34c can remarkably inhibit replication and expression of HBV DNA, inhibit proliferation of liver cancer cells and promote apoptosis of liver cancer cells, and the researches show that the miR-34c can be helpful for early diagnosis and prognosis and treatment of the HBV related liver cancers, so the miR-34c can be used for preparing medicaments or health-care products for treating or preventing the liver cancers, particularly the primary liver cancers caused by HBV infection.
EP1595871A2 Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.
US20100143454 Flavivirus NS5A Proteins For the Treatment of HIV GB virus C (GBV-C or hepatitis G virus) is a flavivirus that frequently leads to chronic viremia in humans. The invention provides compositions and methods involving a -GBV-C NS5A peptide or polypeptide for inhibiting and treating HIV infections.
US20110039861 Cyclic azaindole-3-carboxamides, their preparation and their use as pharmaceuticals The present invention relates to cyclic azaindole-3-carboxamides of the formula I, wherein A, R, R10, R20, R30, R40, Y1, Y2, Y3, Y4, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
CN103041254A Asthma-relieving, cough-relieving and sputum-reducing paste The invention relates to an asthma-relieving, cough-relieving and sputum-reducing paste which is characterized in that an ointment of compound preparations of roasted semen brassicae, rhizoma corydalis, Euphorbia kansui, asarum, pericarpium zanthoxyli, pericarpium zanthoxyli, rhizoma kaempferiae, radix angelicae, Platycodon grandiflorum, polygala tenuifolia, smoked plum, radices sileris, radices stellariae dichotomae, Schisandra chinensis, hematoxylon and borneol is arranged on a tray formed by aluminum-foil paper. Four asthma-relieving, cough-relieving and sputum-reducing pastes in rectangular strips form a treatment group and are respectively pasted to bladder meridian, acupoint, feishu point, faint point, heart point, and liver point on the back of the patient when used to treat asthmatoid bronchitis, chronic bronchitis, and bronchial asthma. The asthma-relieving, cough-relieving and sputum-reducing paste provided by the invention has the advantages that the deficiency that blisters or even remarkable scars appear on the skin due to local reaction by using a medicinal extract recorded by Zhangshi Yitong for a long time is overcome, and the effect on treating symptoms of asthmatoid bronchitis, chronic bronchitis and bronchial asthma is optimal; clinical tests from 1990 to 2011 show that the paste is free from remarkable toxic and side effects and adverse reactions, and the general efficiency can be over 92%.
CN102329362A Ursolic acid derivative chemically modified by polyethylene glycol and preparation method of ursolic acid derivative The invention relates to an ursolic acid derivative chemically modified by polyethylene glycol and a preparation method of the ursolic acid derivative. In the method, a novel ursolic acid derivative with anticancer activity is developed by modifying 28 bits of carboxyl of ursolic acid with butanedioic anhydride, ethylene diamine and polyethylene glycol. As proved by a pharmacological test, the ursolic acid derivative has remarkable in-vitro suppressing capabilities on human liver cancer HepG2 cells, human stomach cancer AGS cells, human stomach cancer BGC-823 cells and human prostatic csarcinoma PC-3 cells.
WO2013068439A1 4-amino-5-oxo-7,8-dihydropyrimido[5, 4 -f] [1, 4] oxazepine compounds as dgat1 inhibitors Described herein are compounds of formula (I). The compounds of formula (I) act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
EP1328269B2 Association of a cb1 receptor antagonist and sibutramin for treating obesity The invention concerns the association of the CB1 receptor antagonist and a sibutramin, pharmaceutical compositions containing same and use thereof for treating obesity.
US20100285038 Factor Involved in Metastasis and Uses Thereof The present invention is related to a nucleic acid coding for a factor involved in a biological process, whereby the process is a PI 3-kinase pathway regulated process, preferably a process selected from the group comprising glucose metabolism, amino acid and glucose deprivation processes, diabetes, wound healing, stress response, apoptosis, metastasis, tumorigenesis, cell migration, cell motility in extracellular matrix and cell growth in extracellular matrix, and the factor is a polypeptide comprising an amino acid sequence according to SEQ ID. NO. 1 or a polypeptide having a sequence according to databank entries gi 9506687 or NP_061931, preferably NP_061931.1.
US20080057133 Preparation of Aqueous Clear Solution Dosage Forms with Bile Acids Compositions for pharmaceutical and other uses comprising clear aqueous solutions of bile acids which do not form any detectable precipitates over selected ranges of pH values of the aqueous solution and methods of making such solutions. The compositions of the invention comprise water; a bile acid in the form of a bile acid, bile acid salt, or a bile acid conjugated with an amine by an amide linkage; and either or both an aqueous soluble starch conversion product and an aqueous soluble non-starch polysaccharide. The composition remains in solution without forming a precipitate over a range of pH values and, according to one embodiment, remains in solution for all pH values obtainable in an aqueous system. The composition, according to some embodiments, may further contain a pharmaceutical compound in a pharmaceutically effective amount. Non-limiting examples of pharmaceutical compounds include insulin, heparin, bismuth compounds, amantadine and rimantadine
EP1720864B1 Benzimidazol substituted thiophene derivatives with activity on ikk3 A compound of Formula (I): and compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such benzimidazole derivatives are potentially useful in the treatment of diseases associated with inappropriate I-kappa-B kinase-3 (IKK3) (also known as I-kappa-B kinase epsilon (IKKϵ) or inducible I-kappa B kinase (IKKi)) activity.
WO2014061752A1 Compound; tautomer and geometric isomer thereof; salt of said compound, tautomer, or geometric isomer; method for manufacturing said compound, tautomer, isomer, or salt; antimicrobial agent; and anti-infective drug A compound characterized in being represented by any of general formulae (1) to (5); a tautomer or a geometric isomer thereof; a salt of the compound, tautomer, or geometric isomer; and the like. (In the formulae, X1 represents a single bond or a C1-8 alkylene group; Y1 represents a single bond, -O-, -NHCO-, etc.; Z1 represents a C8-30 alkyl group optionally having a halogen atom; X2 represents a single bond, -CO-, etc.; Y2 represents a hydrogen atom or an optionally-substituted C1-30 hydrocarbon group; Z2 represents a C5-30 hydrocarbon group optionally having a halogen atom; X3 represents a single bond, or -NH-; Y3 represents -O-, -NH-, etc.; X4 represents a C1-8 alkylene group; Z represents a hydrogen atom, a halogen atom, a C1-6 alkoxy group, or a C1-20 hydrocarbon group; R1 represents an optionally-substituted C1-30 hydrocarbon group; and Z3 represents a halogen atom, a C1-6 alkoxy group, or a C1-20 hydrocarbon group).
EP2683376A2 Methods for treating diseases using isoindoline compounds Methods of treating a disease selected from dermatomyositis, prurigo nodularis, pyoderma gangrenosum, alopecia areata, hidradenitis suppurtiva, rosacea, lichen planus, giant cell arteritis, Sjogren's syndrome, gout, chronic prostatitis, posterior uveitis, vulvodynia and interstitial cystitis in a human are disclosed. Specific methods encompass the administration of (+)-2-[l-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4- acetylaminoisoindoline-l,3-dione, cyclopropyl {2-[(15)-l-(3-ethoxy-4-methoxyphenyl)-2- (methylsulfonyl)ethyl]-3-oxoisoindolin-4-yl}carboxamide or a combination thereof, or a pharmaceutically acceptable prodrug, metabolite, polymorph, salt, solvate or clathrate thereof.
CN103110609A Film coating agent for treating dental ulcer and preparation method thereof The invention discloses a film coating agent for treating dental ulcer and a preparation method thereof. The film coating agent comprises the following raw materials: iodine chitosan, hydroxypropyl methyl cellulose, glacial acetic acid, polysorbate-20, glycerol, absolute ethyl alcohol, potassium iodate and purified water. The method for preparing the film coating agent comprises the following steps: (1) weighting the materials according to formula mass; (2) adding glacial acetic acid, polysorbate-20, glycerol and partial purified water to iodine chitosan, and then completely and uniformly stirring until complete dissolution; (3) adding hydroxypropyl methyl cellulose, and stirring overnight so as to completely dissolve, then adding absolute ethyl alcohol and uniformly stirring; (4) dissolving potassium iodate with a small amount of purified water, adding to the material in the former step, and then uniformly stirring; (5) adding the rest purified water to 100%, and then uniformly stirring; and (6) filling, and packaging to obtain the product. The film coating agent for treating the dental ulcer disclosed by the invention has the advantages of good stability, better sterilizing effect and convenience for use, so that the film coating agent can be applied clinically and can be used for treating dental ulcer.
CN102000090A Compound preparation with Budesonide and Arformoterol as active ingredients The invention relates to a compound preparation with Budesonide and Arformoterol as active ingredients and application thereof. The compound preparation is a medical composition which is formed by mixing Budesonide and Arformoterol used as active ingredients with pharmaceutically acceptable auxiliary materials; and the compound preparation is developed into an aerosol which is administrated through an oral cavity according to the technical means in the invention. The compound preparation has the advantages of fast absorption, quick effect acting and the like, is convenient to use and can be used for treating various asthma, COPD (Chronic Obstructive Pulmonary Disease) and other diseases.
US20070238684 For an improved in vitro and in vivo transformation of particular cells, for example for somatic gene therapy; diagnosis, increased infectivity for cells of low susceptibility, such as haematopoietic cells The invention relates to a structural protein of adeno-associated virus (AAV) which comprises at least one mutation which brings about an increase in the infectivity of the virus.
CN102796066A Flavone compound and preparation method and application thereof The invention discloses a flavone compound and a preparation method and an application thereof. The flavone compound is separated from rose, is shown as a molecular formula C20H18O7, and has a structure shown in the specifications. The preparation method of the flavone compound is characterized in that: rose is taken as a raw material, and extract extraction, silica gel column chromatography, petroleum ether-ethyl acetate column chromatography and high-pressure liquid phase chromatography separation steps are performed. The method comprises the following specific steps of: smashing rose, ultrasonically extracting with 90-99 percent ethanol, combining extracting solutions, filtering, and concentrating under reduced pressure to obtain extract; loading the extract onto a column with a silica gel dry method for performing silica gel column chromatography; gradually eluting with a chloroform-methanol solution in the volume ratio of 20:1-1:1, and combining the same parts; gradually eluting a 9:1 part with a petroleum ether-ethyl acetate solution in the volume ratio of 9:1-0:1, collecting every part of eluent, and concentrating; and further separating and purifying a 7:3 part with high-pressure liquid phase chromatography to obtain the flavone compound. The compound is simple in structure, is easy for realizing manual synthesis, has high activity, and can be taken as a pilot compound of an antitumor medicament.
EP1700602A1 Pharmaceutical composition for use in hormone replacement therapy One aspect of the invention is concerned with the use of an estrogenic component selected from the group consisting of: substances represented by the following formula in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; and no more than 3 of R1, R2, R3, R4 are hydrogen atoms; derivatives of these substances wherein the hydrogen atom of at least one of the hydroxyl groups in said formula has been substituted by an acyl radical of a hydrocarbon carboxylic, sulfonic or sulfamic acid of 1-25 carbon atoms, tetrahydrofuranyl, tetrahydropyranal, or a straight or branched chain glycosidic residue containing 1-20 glycosidic units per residue; and mixtures thereof; in the preparation of a composition for use in a method of hormone replacement therapy, which method comprises non-orally administering to a person in need of such a therapy an effective amount of the estrogenic component without adjunctive progestogen or anti-progestogen treatment, said composition containing no progestogen or anti-progestin. Another aspect of the invention relates to a drug delivery system for enteral or parenteral administration that contains at least 1 µg of the aforementioned estrogenic component and no progestogen or anti-progestin.
US20120114776 Methods for preparing probiotic nanoparticles Various embodiments of the present invention are directed toward a method for preparing probiotic nanoparticles from natural sources, comprising performing a biological preparation phase such as isolating any cells derived from either prokaryote or eukaryote cells, performing a chemical preparation phase such as performing an enzymatic procedure (or heating, or chemicals) for killing or obtaining cell derived ingredients, performing a physical preparation phase such as performing ultrasonication, and performing a formulation preparation phase such as powderized drying.
WO2011096688A3 Composition for improving scalp and hair health comprising a dibenzo-p-dioxin derivative The present invention relates to a composition for improving scalp and hair health comprising a dibenzo-p-dioxin derivative as an active ingredient. The composition for improving scalp and hair health both safely and effectively suppresses Malassezia resista proliferation, oxidative stress and inflammatory reaction in the scalp and hair, and thereby provides outstanding effects in preventing hair loss, promoting hair growth, preventing dandruff, alleviating scalp inflammation, and suppressing scalp itching. The composition of the present invention also effectively prevents dirtiness due to hair-surface breakdown and microorganisms, and thereby provides an effect whereby the hair is kept looking healthy and attractive.
WO2005013955A2 Topical composition comprising terbinafine and hydrocortisone The invention relates to topical pharmaceutical compositions comprising terbinafine and hydrocortisone. Said compositions exhibit beneficial antimycotic properties, especially against dermatophytes.
WO2007023141A1 N-oxides as prodrugs of piperazine & piperidine derivatives The present invention relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The invention also relates to the use of compounds disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
WO2014064711A3 Methods of administering raltegravir and raltegravir compositions The disclosure is related to amorphous raltegravir and the solid oral dosage forms of amorphous raltegravir that are of lower dosage than the commercially available reference dosage form. Provided herein are a pharmaceutical solid oral dosage form composed from (a) 300 mg of amorphous raltegravir or an equivalent amount of a pharmaceutically acceptable salt thereof; (b) a polymer; and (c) a pharmaceutically acceptable excipient and a method of reducing adverse effects of raltegravir administration in a human subject, comprising administering to the human subject a solid oral dosage form comprising 300 mg of amorphous raltegravir or an equivalent amount of a pharmaceutically acceptable salt thereof.
CN101427998B Astragalus polysaccharide calcium phosphate nano-paclitaxel composite injection, and preparation method The invention relates to astragalus polyose calcium phosphate nano taxol complex injection and a preparation method and the application thereof. 100 mL of injection comprises the following components: 0.01 to 1 g of astragalus polyose calcium phosphate nano to particles, 1.0 to 50 mg of taxol, 0 to 5.0 g of osmotic pressure regulator and appropriate amount of water. The pH value of the injection is 6.0 to 7.5. The preparation method comprises the following steps: blending the taxol with absolute ethyl alcohol to form taxol-absolute ethyl alcohol solution; blending the astragalus polyose with ultrapure water to form astragalus polyose solution; performing stirring and ultrasonic processing to the solution, rejecting the supernatant fluid after separation, and after depositing, drying and sterilizing, obtaining astragalus polyose calcium phosphate nano taxol complex granules used for injection, then adding the osmotic pressure regulator into the water for injection, and mixing with the astragalus polyose calcium phosphate nano taxol complex granules; after ultrasonic processing, astragalus polyose calcium phosphate nano taxol complex injection is formed. The complex injection can beused for the treatment or auxiliary treatment of tumor.
US20090281123 Novel thiazolo (4,5-d) pyrimidine compounds novel compounds The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
CN102971305A Heterocyclic antiviral compounds Compounds having the formula I wherein R1, R2, R3 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
US20110092517 Use of PPAR Delta Ligands for the Treatment or Prevention of Inflammation or Energy Metabolism/Production Related Diseases Provided herein are methods for treatment, prevention, or amelioration of one or more symptoms of a disease or condition related to disorders of insulin and/or glucose metabolism, inflammatory conditions, mitochondrial disease, muscle disorders, or pulmonary disorders, involving administering a PPARδ agonist or a pharmaceutical composition comprising a PPARδ agonist. In one embodiment, the disease or condition is selected from myopathy, inflammatory vascular diseases, Parkinson's and Alzheimer's diseases, systemic inflammatory disorders, renal ischemia, inflammatory rheumatic disorders, and inflammatory diseases of the lung. In another embodiment, methods for increasing oxidative muscle fibers, reducing mitochondria disease, decreasing insulin resistance, decreasing plasma glucose, or decreasing weight, involving administering a PPARδ agonist or a pharmaceutical composition comprising a PPARδ agonist, are provided.
WO2009077736A3 A medicament comprising a parasympathetic agonist and a sympathetic antagonist or a sympathetic agonist A medicament for topical administration to a human or animal eye comprises at least two pharmacologically active agents. One of the active agents is a parasympathetic agonist, such as pilocarpine, and the other active agent is either a sympathetic antagonist such as dapiprazole or thymoxamine, or a sympathetic agonist such as brimonidine or iopidine. The medicament is preferably in the form of a liquid composition, such as eye drops, or a gel or ointment and may comprise a slow-release composition. The medicament acts to improve visual acuity for a period of several hours, and may be beneficial in cases of presbyopia, myopia, hypermetropia, astigmatism and/or impaired night vision.
CN102603824A New 3'-azido daunorubicin-13-thiosemicarbazone compound with cancer resistance and preparation method thereof The invention discloses a new 3'--azido daunorubicin-13-thiosemicarbazone compound with cancer resistance and a preparation method thereof. The preparation method comprises the following specific steps: reacting 3'-azido daunorubicin with various thiosemicarbazide to synthesize the new 3'-azido-daunorubicin-13-thiosemicarbazone compound. The compound shows high activity in the activity test of cancer cells.
CN103462967A Application of Incarviatone A in anti-herpes virus medicaments The invention discloses an application of Incarviatone A in preparation of anti-herpes virus medicaments. Experiments prove that the Incarviatone A has a prominent inhibiting effect on herpes simplex virus-1 (HSV-1) and herpes simplex virus-2 (HSV-2), which hints that the Incarviatone A has a potential application value in the field of treatment of herpes virus infected diseases. The application provides experiment basis for clinically applying the Incarviatone A to treat the herpes virus infected diseases, provides certain guiding significance for researching anti-HSV-1 and anti-HSV-2 virus medicaments, and has an important reference value.
US20120093938 Orally disintegrating tablets comprising diphenhydramine The compositions of the present invention comprise a therapeutically effective amount of particles consisting of diphenhydramine or pharmaceutically acceptable salts thereof, optionally in combination with another drug such as pseudoephedrine, or phenylephrine and hydrocodone, in combination with rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol and/or a saccharide. These compositions are useful in treating the symptoms of one or more diseases or conditions in which diphenhydramine (alone or in combination with one or two other drugs) is a therapeutically effective, e.g. allergic rhinitis, sinusitis, upper respiratory tract infections, motion sickness, Parkinson's disease, insomnia, the common cold, and nighttime pain management, particularly for subjects or patients with dysphagia, and people ‘on the move’.
WO2006023242A1 Benzoxazepine derivatives as selective estrogen receptor modulators The present invention is directed to novel benzoxazepine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and diseases mediated by an estrogen receptor.
CA2296492C Use of compositions containing the combination of acetaminophen, aspirin and caffeine to alleviate the pain and symptoms of migraine The invention provides a safe and economical nonprescription combination of acetaminophen, aspirin and caffeine (APAP/ASA/CAF) for use in treating migraine pain and the cluster of symptoms characteristic of migraine attack, such as nausea, photophobia, phonophobia and functional disabilities. In accordance with the present invention, the use of the APAP/ASA/CAF combination is also effective in aborting the prodrome phase of a migraine attack, prior to the onset of the migraine-associated symptoms, aborting the symptoms of migraine attack prior to the onset of severe, throbbing migraine pain, and aborting migraine pain after a migraine has fully developed. In accordance with the present invention, the efficacy of the APAP/ASA/CAF combination treatment in reducing and eliminating migraine pain is at a parity with the efficacy of sumatriptan, a known, but dissimilar, anti-migraine agent, used at similar dosing regimens. Use of the APAP/ASA/CAFcombination composition treatment at the unit dose also advantageously reduces/obviates the need of the migraine sufferer to re-dose or re-medicate at the end of the dosing period in accordance with the present invention.
CN102058887A Application of P2Y4 receptor stimulant in preparing medicaments for treating Alzheimer's disease The invention provides application of a P2Y4 receptor stimulant in preparing medicaments for treating the Alzheimer's disease. The application of the P2Y4 receptor stimulant in preparing medicaments for treating the Alzheimer's disease has the beneficial effects that the P2Y4 receptor stimulant can be used for effectively promoting the pinocytosis to beta-amyloid polypeptide of microglial cells so as to relieve and even cure the Alzheimer's disease; and the P2Y4 receptor stimulant has lower toxicity and low risk and is clinically applied to treating various diseases, thus the P2Y4 receptor stimulant has good application prospect in treating the Alzheimer's disease.
EP2129368B1 Combination for use in the treatment of inflammatory disorders There is provided combination products comprising (a) suplatast, or a pharmaceutically-acceptable salt or solvate thereof; and (b) a statin, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in the treatment of atherosclerosis and related conditions.
US20050148527 Catalytic nucleic acids; ribozymes; translation inhibition; gene expression inhibition; for treating cardiovascular disease; for neovascularization induction in heart tissue The present invention provides DNAzymes and ribozymes that specifically cleave PAI-1-encoding mRNA. The present invention also provides antisense oligonucleotides that specifically inhibit translation of PAI-1-encoding mRNA. The invention also provides various methods of inhibiting the expression of PAI-1, and methods of treating diseases by such. Finally the invention provides pharmaceutical compositions containing the instant DNAzymes, ribozymes, antisense oligonucleotides, or other inhibitors of PAI-1 expression as active ingredients.
US7125858 Hyaluronic acid in the treatment of cancer The present invention relates to a composition and method comprising purified HA, a second anti-neoplastic agent and a pharmaceutically acceptable carrier, wherein the purified HA and the second anti-neoplastic agent are administered to a mammal having cancer in an amount effective to treat the cancer.
US20100152229 Process for the Synthesis of Moxifloxacin Hydrochloride A new polymorph of moxifloxacin hydrochloride is described, together with a method for making the polymorph. In addition, new intermediates in the formation of moxifloxacin hydrochloride are described, having formulas (1) and (II):
CN101332199A Anticancer composition containing phosphoinositide 3-kinase inhibitor and topology enzyme inhibitor An anti-cancer combination containing a phosphoinositide3-kinase inhibitor (PI3Ki) and/or a topoisomerase inhibitor is a sustained-release injection, which contains a sustained-release microsphere and a menstruum. The sustained-release microsphere contains PI3Ki and/or topoisomerase inhibitor and sustained-release auxiliary materials; the menstruum is an ordinary menstruum or a special menstruum containing a suspending agent. The viscosity of the suspending agent is 100cp to 3000cp (at the temperature of 20 DEG to 30 DEG) and the suspending agent is selected from carboxymethylcellulose sodium, etc. The sustained-release auxiliary materials are selected from a polyphosphonate copolymer of p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP/TC), p(BHET-EOP/TC ), p(BHDPT-EOP/TC), p(BHDPT-EOP/TC), p(CHDM-HOP) or p(CHDM-EOP), and the like, or a copolymer of polyphosphate ester and polylactic acid, polifeprosan, dienoic fatty acid or decanedioic acid, a copolymer or a mixture of p(erucic acid dimer-decanedioic acid) or a copolymer or a mixture of p(boletic acid-decanedioic acid). The anti-cancer combination is also made into a sustained-release implanting agent, which can be injected or placed in or around tumor to maintain the effective medicine density for more than 40 days. The anti-cancer combination can also obviously reduce the general reaction of the medicine and selectively enhance the curing effect of non-operational therapies such as radiotherapy and chemotherapy.
EP1499307A1 Low-pressure mercury vapor discharge lamp Low-pressure mercury vapor discharge lamp provided with a discharge vessel (10) which encloses enclosing a discharge space (11) provided with a filling of mercury and a rare gas in a gastight manner. The inner wall of the discharge vessel (10) is provided with a transparent layer (16) and a luminescent layer (17). According to the invention, the luminescent layer (17) is provided with a further transparent layer (18). Preferably, both transparent layers (16, 18) comprise an oxide of scandium, yttrium, or a further rare-earth metal, and/or a borate or phosphate of an alkaline-earth metal, and/or of scandium, yttrium, or a further rare-earth metal. Preferably, the alkaline-earth metal is calcium, strontium, and/or barium. The further rare-earth metal is preferably lanthanum, cerium, and/or gadolinium. The oxide is preferably Y2O3 or Gd2O3. The lamp according to the invention has a comparatively low mercury consumption.
EP1856090B1 Substituted thiophene derivatives as glucagon receptor antagonists, preparation and therapeutic uses The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
US20120027870 Novel Markers for Bladder Cancer Detection A method of detecting a predisposition to, or the incidence of, bladder cancer in a sample comprises detecting an epigenetic change in at least one gene selected from FOXE1 and GATA4. Detection of the epigenetic change is indicative of a predisposition to, or the incidence of, bladder cancer. The sample comprises nucleic acid molecules from bladder cells. The methods may be used to select treatments and patients for treatment. Related kits include primers allowing the methylation status of the genes to be determined.
WO2013168007A1 Compositions and methods for the treatment of cardiovascular and neurological diseases The invention relates to the compounds of formula (I), formula (II) and formula (III) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), formula (II) or formula (III) and methods for the treatment of cardiovascular and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment: of hyperglycemia, insulin resistance, diabetes mellitus, diabetes insipidus, type 1 diabetes, type 2 diabetes, microvascular complications, macrovascular complications, lipid disorders, prediabetes, obesity, arrhythmia, myocardial infarction, stroke, neuropathy, renal complications, hypertriglyceridemia, cardiovascular complications, postprandial hyperglycemia, depression, Alzheimer's disease, Parkinson's disease, Huntington's disease, inflammation, Crohn's disease, inflammatory bowel disease and obesity.
US20050148576 Dibenzo[b.f]oxazolo-azulines, -oxepines and -thiepines; antiinflammatories; analgesics The present invention relates to derivatives of 1-oxa-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumour necrosis factor-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.
EP1911358A1 New composition for improving skin quality and a process for preparing the same The present invention relates to a composition comprising, as active substance, a mixture of at least one polyunsaturated fatty acid, different from polyunsaturated fatty acid derived from milk, polyphenols, milk proteins and lactic bacteria, and said composition having a water content of at least 50% by weight; and wherein the said polyunsaturated fatty acid presents an increased bioavailability compared with the one of the polyunsaturated fatty acid alone.
CA2349715C Electrotransport device including a compatible antimicrobial agent A transdermal electrotransport drug delivery device (10) having an anode, a cathode and a source of electrical power electrically connected to the anode and the cathode. The cathode includes a cathodic electrode (24) and a cathodic reservoir (28) comprised of a housing composed of a polymeric material and an aqueous medium in contact with the housing. The aqueous medium includes i) a drug or an electrolyte salt or a mixture thereof and ii) a cetylpyridinium salt in an amount sufficient to inhibit microbial growth in the aqueous medium. The polymeric material is compatible with the cetylpyridinium salt. A process is also provided wherein when electric current flows from the source of electrical power so that the drug is transdermally delivered to the patient by electrotransport from the anodic reservoir, the cetylpyridinium salt is not transdermally delivered to the patient by electrotransport from the cathodic reservoir.
US20100173860 Purifications of Pomegranate Ellagitannins and Their Uses Thereof Compositions of purified and biologically active ellagitannins are provided by separation from pomegranate husk using a method of extraction and purification using a solid polymeric adsorbent and the uses of the said compounds
CN102526071A Application of Ppt for resisting cognition and learning and memorial dysfunctions The patent application is divisional application, and the original application number is 200810103061.5. The invention discloses the application of ginsenoside Rg1, Rh1 and Ppt for resisting cognition and learning and memorial dysfunctions and particularly relates to the application of the ginsenoside Rg1and/or metabolin Rh1 and/or Ppt in preparation of pharmaceuticals and health care products for preventing, relieving and/or curing diseases or symptoms which are capable of causing a cognitive dysfunction and/or learning and memorial dysfunctions, especially Alzheimer's disease (AD), and the application performed in the preparation of the pharmaceuticals and the health care products for improving a cognitive function and learning and memorial functions.
WO2008035001A2 Composition for the treatment of amyotrophic lateral sclerosis The invention relates to the use of a composition for controlling the evolution of amyotrophic lateral sclerosis, characterised in that it comprises at least: a conjugate of poly-lysine and at least one anti-oxidant, and a conjugate of poly-lysine and at least one fatty acid. The invention also relates to a particular composition for controlling the evolution of amyotrophic lateral sclerosis.
US7402569 Combining such as sulforaphane with glucosinolate component; economical food additive or dietary supplement The present invention relates to methods of preventing or inhibiting the growth of Helicobacter through the use of a composition that comprises a glucosinolate, an isothiocyanate or a derivative or metabolite thereof. The present invention also relates to methods of preventing or treating persistent chronic gastritis, ulcers and/or stomach cancer in subjects at risk for, or in need of treatment thereof.
EP1254133B1 Indol-3-yl derivatives and their use as integrin inhibitors Indol-3-yl derivatives of general formula (I), wherein A, B, X, R?1, R2, R3, R4, R5¿, n or m have the meanings given in Claim 1, and the physiologically unobjectionable salts or solvates thereof are integrin inhibitors and can be used for combating thrombosis, myocardial infarcts, coronary heart diseases, arteriosclerosis, inflammations, tumours, osteoporosis, rheumatic arthritis, macular degenerative diseases, diabetic retinopathy, infections and restenosis after angioplasty or in the event of pathological actions which are maintained or propagated by angiogenesis.
CN1827091A Medicinal composition containing backuchiol for treating female breast cancer This invention supplies new uses of single-methoxsalen compounds or methoxsalen-containing extractants used in curing or preventing breast cancer. A concrete example is a medicine composition for curing or preventing breast cancer. The type of the medicine compositions can be skin absorption, oral administration, injection or slow release. At the same time this invention opens out new uses of methoxsalen compounds or methoxsalen-containing extractants in curing or preventing osteoporosis.
CN101245061B N-(5-amido-2-methyl phenyl)-4-(3-pyridinyl)-2-aminopyrimidine nitric oxide donating derivant, production method and uses thereof The invention provides an N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine derivative, in particular to a compound which is obtained by connecting the N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine with an NO(nitric oxide) supply body for nitrate esters by ester bonds or amide bonds. The compound is obtained by coupling the N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine and the corresponding NO supply body for nitrate esters by different connecting groups for carrying out substitution reaction. The dual-coordination anti-tumor mechanism demonstrates good functions on inhibiting the cell apoptosis or inducing the apoptosis of tumor cells.
CN1872120A Troche of health products, preparation and application A composite health-care food in the form of tablet for delaying sanility, relieving fatigue and improving immunity is proportionally prepared from aqueous extract of ganoderma, superfine ginseng powder, superfine ganoderma powder, wall-broken ganoderma spore powder, VE, adhesive and flowing aid. Its preparing process is also disclosed.
CN101040863B Medicine monocase compound for treating alzheimers disease The invention discloses a Chinese monomer compound for treating Alcemu disease, formed by 1.0-50mol panaxoside Rg, 1.0-50mol panaxoside Re, 11.0-50mol panaxoside RB, and 1.0-50mol polygalin Pre-Se, to be prepared by general method into the injection, oral, capsule, tablet or extractive whose main components are aforementioned Chinese drugs. Research has proved that Chinese monomer compound can treat Alcemu disease. The inventive compound has less components, easy separation and extraction, with wide application.
US20120142650 Method for treating lung disease Methods of treating lung diseases comprising administering inducers of NAD(P)H:quinone oxidoreductase 1 (NQO1) are disclosed. Inducers of NQO1 include naphthoquinones such as β-lapachone. Methods of predicting whether a subject with a lung disease will respond to treatment with a naphthoquinone are also described herein.
US20080219988 Polypeptide comprising major histocompatibility complex epitopes for targeting and destroying tumor cells Compositions and methods for the therapy and diagnosis of cancer, particularly prostate cancer, are disclosed. Illustrative compositions comprise one or more prostate-specific polypeptides, immunogenic portions thereof, polynucleotides that encode such polypeptides, antigen presenting cell that expresses such polypeptides, and T cells that are specific for cells expressing such polypeptides. The disclosed compositions are useful, for example, in the diagnosis, prevention and/or treatment of diseases, particularly prostate cancer.
US20050019386 In mixture of membrane-forming amphiphiles subjected to high pressure homogenization or ultrasound; contain immunomodulator, cyclosporin, and/or at least one cytokine or polyethylene glycol-cytokines The invention relates to pharmaceutical preparations suitable for oral application of liposomally encapsulated Taxol, its derivatives and Taxan. Preferably, they additionally contain at least one immuno-modulator, preferably Cyclosporine, and/or at least one cytokine, preferably PEG cytokines.
CN102580022A Process for combination of Chinese and western medicinal dexamethasone and absorption of aquatic medicines by skin anatripsis and dietary therapy The invention relates to a process for combining shinyleaf pricklyash root tinisulphur dexamethasone by the skin absorption of aquatic medicines and dietary therapy. The process is characterized in that 1, the medicines have the effects of purging fire for removing toxin, tonifying kidney and nourishing marrow, clearing heat, inducing diuresis and treating stranguria, tonifying qi and yin and promoting blood circulation to remove meridian obstruction, nourishing yang, tonifying kidney, nourishing heart and soothing nerves, tonifying kidney and dredging collaterals, clearing away liver-fire, calming liver, regulating qi and reducing pathogenic fire, warming middle-jiao, eliminating cold, regulating vital energy, harmonizing stomach and relieving pain, purgating fu-organs and removing stagnancy and obstruction, soothing liver-qi stagnation, reducing phlegm, resolving masses, invigorating qi and blood, transporting spleen and stomach, inhibiting the synthesis of lymph C and deoxyribonucleic acid (DNA) and the ingestion of mitosis macrophage C on antigens and contributing to the improvement of local blood circulation by the anatripsis of the aquatic medicines and preventing and treating diseases by glycerol, fancy soap, ointment, edible rice, vegetable soup and food such as health-care tea, acidic drinks, yoghourt, cheese and the like; and 2, aloes have a special effect of treating fungus and removing freckles.
US8377481 Apparatus and method to generate a mixture of hydrogen peroxide gas and a carrier gas This relates to a method to generate a mixture of Hydrogen Peroxide gas and a Carrier gas, consisting in passing a dry Carrier gas through a solution of Hydrogen Peroxide.
WO2014139465A1 Novel pyrimidine and pyridine compounds and their usage The present invention relates to novel pyrimidine and pyridine compounds of formula (I) or a pharmaceutical acceptable salt thereof, wherein R1, R2, R3, R4, R5, X, Y and G are as defined in the description, to pharmaceutical compositions containing them, a process for preparing them, and their use in therapy of a disease responsive to inhibition of FGFR, for example, cancer.
US7205108 Trp8, Trp9 and Trp10, novel markers for cancer The present invention relates to gene expression in normal cells and cells of malignant tumors and particularly to novel markers associated with cancer, Trp8, Trp9 and Trp10, and the genes encoding Trp8, Trp9 and Trp10. Also provided are vectors, host cells, antibodies, and recombinant methods for producing these human proteins. The invention further relates to diagnostic and therapeutic methods useful for diagnosing and treating a tumor.
WO2005123703A3 Alkynyl derivatives as modulators of metabotropic glutamate receptors The present invention relates to novel compounds of formula (I) wherein W, n, X and W’ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors - subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
US7585966 Directed against accessible regions in the telomerase ribonucleoprotein; cancer This invention provides inhibitory polynucleotides, such as antisense molecules, directed against accessible regions in the telomerase ribonucleoprotein. The polynucleotides are useful for inhibiting the activity of telomerase in cells and for treating cancer.
WO2013162048A1 Injectable preparation An object of the present invention is to provide a storage-stable injectable preparation comprising a composition comprising a poorly soluble drug as an active ingredient and a dispersion medium. Another object of the present invention is to provide a compact, lightweight prefilled syringe by filling a syringe with the injectable preparation. The present invention provides an injectable preparation comprising a composition comprising a poorly soluble drug, a dispersion medium, and a specific suspending agent, the composition having a viscosity of 40 pascal-seconds or more in at least one point in the shear rate range of 0.01 to 0.02 s-1 and having a viscosity of 0.2 pascal-seconds or less in at least one point in the shear rate range of 900 to 1,000 s-1, as measured.
US20050112556 Drug screening; endogenous human retrovirus; protein or peptide expressed by said retrovirus The invention relates to a process for the diagnosis of a human autoimmune disease, including presymptomatic diagnosis, said human autoimmune disease being associated with human retrovirus (HERV) having Superantigen (SAg) activity, comprising specifically detecting in a biological sample of human origin at least one of the following: (I) the mRNA of an expressed human endogenous retrovirus having Superantigen (SAg) activity, or fragments of such expressed retroviral mRNA, said retrovirus being associated with a given autoimmune disease, or (II) protein or peptide expressed by said retrovirus, or (III) antibodies specific to the protein expressed by said endogenous, or (IV) SAg activity specifically associated with said endogenous retrovirus, detection of any of the species (I) to (IV) indicating presence of autoimmune disease or imminent onset of autoimmune disease.
CN101716133A Aseculin ophthalmic gel and production method and application thereof The invention discloses aseculin ophthalmic gel and a production method and the application thereof; the aseculin ophthalmic gel provided by the invention is prepared by the following raw materials by mass parts: 4.8-5.2 parts of aseculin, 35-45 parts of boric acid, 380-420 parts of hydroxypropyl methyl cellulose, 180-220 parts of sodium alga acid, 23-27 parts of dimethyl fumarate and 49300-49350 parts of water; by adopting the formulation selection and preparation technology, the aseculin is produced into ophthalmic gel preparation for treating inflammation of eye part; the extraction method of the aseculin can lead the purity of the product to achieve 99.4 percent; the aseculin ophthalmic gel obtained in the invention is used for treating inflammation of eye part, the invention is firstly proposed and has high comfort degree and extract curative effect.
CN102727579A Pharmaceutical composition for treatment of oral ulcers The invention discloses a pharmaceutical composition for treatment of oral ulcers. The pharmaceutical composition is characterized in that it comprises the following components by weight: 5 parts of chitosan oligosaccharide, 1 part of a Salvia miltiorrhiza extract, and 0.15 part of menthol. The pharmaceutical composition of the invention is applied in wound surface repairing tests, and results show that wound surfaces generally heal and no obvious scar is left. Cell proliferation tests prove that the pharmaceutical composition has a good proliferation effect on cells, and the oral ulcer healing situation is obviously better than that of a control group. The inventor conducts acute toxicity tests on the pharmaceutical composition, and according to the grading standards of acute toxicity, the tested drug can be regarded as non-toxic. Therefore, the pharmaceutical composition of the invention can be used for treatment of oral ulcers, and have great clinical application value.
EP2689779A1 Derivatives of azaindazole or diazaindazole type for treating a cancer overexpressing trk The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.
US20100041616 Formulations for Nonsurgical Exogenous Crosslink Therapy Improved methods and compositions for the treatment of native tissues with crosslinkers are provided. The methods and compositions will find particular use in increasing resistance to tearing, fissuring, rupturing, and/or delamination.
CN103360315A Heterocyclic aryloxyacetyl hydrazone derivative and its preparation method and application thereof The invention relates to a heterocyclic aryloxyacetyl hydrazone derivative as shown in the general formula I and its pharmaceutically acceptable salt, ester or prodrug, its preparation method and an application of a composition containing one or more of the compounds in preparation of drugs for treating and preventing influenza.
EP1272049B1 Method for the fractionation of oil and polar lipid-containing native raw materials using alcohol and centrifugation A process for the production of polar lipid-rich materials and preferably phospholipids. Preferably the polar lipid-rich materials are separated and recovered from native raw materials by extraction with water-soluble organic solvent and use of density separation to separate the resulting mixture.
CN102940607A Injection of piperacillin-sulbactum sodium medicine composition injection and preparation method thereof The invention discloses an injection of a piperacillin-sulbactum sodium medicine composition injection and a preparation method thereof. The injection disclosed herein comprises 1-10 weight parts of piperacillin, 0.5-5 weight parts of sulbactam sodium, 0.4-8 weight parts oflactose, 0.4-8 weight parts of sodium chloride and a proper amount of sodium dihydrogen phosphate for adjusting the pH value of the solution to 7.0. The preparation method comprises the following steps: weighing piperacillin, sulbactam sodium, lactose, and sodium chloride based on the weight parts, using water for injection to dissolve, using the sodium dihydrogen phosphate for adjusting the pH value of the solution to 7.0, then diluting with water for injection to obtain 5000 ml of medicine solution; and filtering the medicine solution by a filtering membrane, drying, conducting sterile crushing, and filling to obtain the injection. According to the invention, the injection has the advantages of high solubility, good stability, etc.
US20090082323 Deuterium-enriched fulvestrant The present application describes deuterium-enriched fulvestrant, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN102697804A Solid molecular iodine disinfectant and preparation method thereof The invention discloses a solid molecular iodine disinfectant and a preparation method thereof. The disinfectant comprises an iodide, an oxidant capable of oxidizing the iodide into iodine molecules, and a pH regulator for regulating the mixture of the iodide and the oxidant to be acidic; the disinfectant consists of a preparation 1 containing the iodide and the oxidant and a preparation 2 containing the pH regulator; and the preparation 1 and the preparation 2 are in a solid state. The disinfectant is high in stability and remarkable in disinfection effect; and due to high water solubility of main agents and auxiliary materials, the disinfectant can be quickly dissolved in water and is safe and convenient to use and carry. Because the raw materials are nontoxic, the disinfectant can be used for soaking disinfection of skin and can also be used for treating various skin diseases caused by bacteria, fungi and viruses.
EP2243776A1 Substituted piperidines and their use for the treatment of diseases related to the histamine H3 receptor A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment of disease and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and dis-orders in which an interaction with the histamine H3 receptor is beneficial.
US20120052079 Compositions, Kits, and Methods for Predicting Anti-Cancer Response to Anthracyclines The present invention is based, in part, on the discovery that amplification of human chromosome 8q22-23 regions and over-expression of 8q22-23 genes (e.g., LAPTM4B and YWHAZ) is associated with and predictive of resistance to anthracycline-type chemotherapy. Accordingly, the invention relates to compositions, kits, and methods for predicting the response of cancer cells, e.g., breast, prostate, lung, ovarian, pancreatic, liver, and colon malignancies to anthracyclines.
US20110262550 Method for treating a skin ailment A method for treating a skin ailment by applying a personal composition from a collapsible dispenser. The collapsible dispenser includes a collapsible bag at least partially surrounded by an elastically deformable member and, optionally, an outer container body. Potential energy is generated by stretching the elastically deformable member, which is used to dispense the composition in lieu of a propellant or pump. The personal care composition may be a skin care composition, an antifungal, or an enzyme inhibiting composition.
CA2783518A1 Bottled ozonated water system A dissolved ozone delivery system comprises a generator for producing gaseous ozone, a bottle for holding a liquid suitable for receiving the gaseous ozone, flow conduits for delivering the gaseous ozone to the bottle and dissolving the ozone into the liquid to form an ozonated liquid, and a multicomponent bottle closure sealing device. The multicomponent bottle closure sealing has several discrete gas flow passageways for channeling the ozone gas into the bottle, venting undissolved gas and delivering the ozonated liquid to an exterior surface for decontamination thereof or medical instruments for sterilization or use in medical or dental procedures.
WO2013122622A1 A method for treating obesity with anti-obesity formulations and omega 3 fatty acids for the reduction of body weight in cardiovascular disease patients (cvd) and diabetics Combinations of one or more anti-obesity drugs with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight comprised of a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA: DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA comprise about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught. EPA + DHA are about 80% of the total formulation and about 89% of the total omega 3 fatty acid content of the composition. The formulation may further contain specific amounts of arachidonic acid (AA) and of omega-3 fatty acids having 18 carbon atoms, including one or more of stearidonic acid (SDA) and alpha-linolenic acid (ALA). The application further teaches methods of administering such combinations, and is directed towards unit dosages of such combinations for the reduction of body weight in cardiovascular disease patients (CVD) and diabetics.
US20080009519 Method of modulating t cell functioning A method of modulating TH1 cell functioning in a mammal, comprising administering to said mammal an effective amount of one or more IDO-mediated tryptophan metabolites or derivatives thereof; or an antagonist thereof.
US20080249162 ATPase inhibitors; anticancer agents; synthesis and chemical intermediates thereto Organic compounds having Formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier can be prepared. Methods of preparing the compounds includes deprotecting protected precursor compounds. Methods of treating cancer or inhibiting ATPase include administering the organic compounds to a subject in need thereof.
CN101538237A Atorvastatin semi-calcium salt butanone co-crystallization substances, preparation and application thereof as HMG-CoA enzyme inhibitor The invention discloses Atorvastatin semi-calcium salt butanone co-crystallization substances, as well as a preparation method and application thereof as an HMG-CoA enzyme inhibitor. Dehydrate formed by combining the Atorvastatin semi-calcium salt butanone co-crystallization substances expressed in a formula (I) with water exists in a stable crystal form (crystal form H). The water solubility (0.46 mg/ml) of the dehydrate is much higher than that of commercially available Atorvastatin semi-calcium salt trihydrate, and the same test method proves that the water solubility of the latter is just 0.198 mg/ml.
WO2013016999A1 Heteroaryl-pyrimidine derivatives, and preparation method therefor and use thereof The present invention relates to heteroaryl-pyrimidine derivatives, and a preparation method therefor and a use thereof. Specifically, the present invention relates to heteroaryl-pyrimidine derivatives represented by General Formula (I) and pharmaceutically acceptable salts thereof, and the use thereof as a cancer treatment agent especially an mTOR inhibitor, wherein definitions of substituents in General Formula (I) are the same as those in the specification.
US7169746 For effecting mental control through psycho-sedation or psycho-stimulation The present invention provides a perfume composition for mental control, the composition containing one or more components acknowledged as having a psycho-sedative effect selected from the group consisting of terpinyl butyrate, γ-nonalactone, acetyl isoeugenol, methyl anisate, terpineol, nerol, chrysanthenone, lyral, lilial, β-phenylethyl alcohol, γ-methyl ionone, Iso E Super, Z-3-hexenyl salicylate, p-methylphenylacetaldehyde, limonene, ocimene, helional, linalyl acetate, geranyl acetate, geraniol, hedione, linalool, citronellol, and γ-hexalactone and/or one or more components acknowledged as having a psycho-stimulative effect selected from the group consisting of piperitone, isoamyl angelate, phenylethyl angelate, cuminyl alcohol, menthalactone, ethyl myristate, and perilla aldehyde. The invention also provides an external composition and daily-use goods, containing the perfume composition for mental control.
WO2012102560A3 Novel 4-0-methylhonokiol derivative and composition containing same as active ingredient for treatment of inflammatory diseases The present invention provides a novel methylhonokiol derivative and a composition containing the same as an active ingredient for the treatment, prevention or improvement of inflammatory diseases. The methylhonokiol derivative of the invention inhibits COX-2(Cyclooxigenase-2) activities, thereby ensuring anti-inflammatory activities. Therefore, the methylhonokiol derivative of the invention can be developed as a therapeutic agent for various inflammatory diseases and as an active component of functional health foods.
CA2398908C Adenosine a2a receptor antagonists for treating and preventing hepatic fibrosis, cirrhosis and fatty liver Fibrosis, hepatic cirrhosis, and fatty liver can be prevented and treated by administering to a subject in need thereof an effective amount of at least one adenosine A2A receptor antagonist or at least one adenosine uptake promoter.
WO2011071981A3 Anti-cytomegalovirus activity of artemisinin-derived dimers Artemisinin-derived monomers and artemisinin dimers are shown to exhibit in-vitro anti-cytomegalovirus (CMV) activity. Artemisinin dimers effectively inhibited CMV replication in human foreskin fibroblasts and human embryonic lung fibroblasts with no cytotxicity at concentrations required for complete CMV inhibition. Artemisinin dimers were found to be potent and non-cytotoxic inhibitors of CMV replication, which indicates their use as therapeutic agents for the treatment of CMV infection in humans.
WO2014079020A1 Pharmaceutical composition used for reducing damage caused by free radicals A pharmaceutical composition used for reducing the damage caused by free radicals is disclosed. The composition comprises at least a metal or its ions, at least a drug or an antioxidant that is carrier-protected/modified, and a drug carrier. Said carrier helps to preserve the anti-oxidative activity, and hence, prevents the decrease of the effect of the antioxidant against free radicals produced in the environment or body fluids and prolongs protection, and may be used for reducing damage caused by radiation and adverse effects induced by chemotherapeutic drugs.
CN102558122A Compound resisting multiple drug-resistant bacteria, and preparation method and application thereof The invention discloses a compound resisting multiple drug-resistant bacteria, and a preparation method and the application thereof. The bacteria resisting compound provided by the invention has a structural formula as shown in a specification, wherein R1 represents H or CH3; R2 plus R3 is equal to O, or R2 represents H and R3 represents OH, or R3 represents OH and R3 represents H. The compound with a brand new structure has good activity for resisting bacteria comprising the multiple drug-resistant bacteria, and is suitable for the studying of lead compounds resisting the bacteria comprising the multiple drug-resistant bacteria and the preparation of drugs resisting the bacterial comprising the multiple drug-resistant bacteria.
US20080254022 Method of Treating Airway Diseases With Beta-Adrenergic Inverse Agonists The use of β-adrenergic inverse agonists provides a new and highly efficient way of treating a number of pulmonary airway diseases, including asthma, emphysema, and chronic obstructive pulmonary diseases. In general, such a method comprises administering a therapeutically effective amount of a β-adrenergic inverse agonist to the subject to treat the pulmonary airway disease. Particularly preferred inverse agonists include nadolol and carvedilol.
WO2013053045A1 Heterocyclic molecules as apoptosis inducers The present document describes novel compounds which may inhibit the activity of anti-apoptotic proteins such as Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases involving a defect in apoptosis, such as, for example, in the treatment of cancer.
EP1795192A2 1-Substituted imidazole derivatives as nos inhibitors N-Heterocyclic derivatives of the following formula: (II) where n, p, A1, R1, R2, R3 and R4 are described herein, as useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
US20110059911 Antiinfective and Antitumoral Compounds Isolated From Tropical Lianas The present invention relates to naphthoquinone derivatives isolated from solid callus cultures from two species of the palaeotropical plant families Dioncophyllaceae and Ancistrocladaceae. It further relates to methods of their production as well as to their use as antiinfective and antitumoral pharmaceuticals.
CN101254197A Applications for curing vertigo medicament The invention discloses an application of glucoseamine in preparing drugs for treating vertigo, and belongs to the technology field of medicines. Through retroactive statistics and clinic experiments on human body, it is proven that glucoseamine has distinct therapeutic and improvement effects on vertigo.
US20110077291 Preparations of Taxanes for Intravenous Administration and the Preparation Method Thereof The present invention relates to the field of medical technology. More specifically, the present invention relates to a preparation of taxanes for intravenous administration, which consists of two parts: a drug solution and an emulsion. Said drug solution consists of paclitaxel or docetaxel, a pH regulator and a solvent for injection, wherein said solvent for injection is an organic solvent. Said emulsion includes a fat emulsion and is composed of oil for injection, an emulsifier, an antioxidant, an isotonic regulator, a stabilizer, a pH regulator and water for injection. When used, the drug solution at the clinical dosage can be added and mixed homogeneously in the emulsion to perform intravenous drip directly; or the drug solution at the clinical dosage can also be firstly added into the emulsion with no less than 5 times volume of the drug solution and then a predetermined amount of normal saline or glucose solution for injection is added to perform intravenous drip. The preparation of the present invention does not contain solubilizer and has advantages of little toxicity, safety, effectiveness, stability and economy. The fat emulsion is also used as a nutritional replenishment, thus achieving a better therapeutic effect. In addition, the normal saline or glucose solution for injection can be used to replace a considerable amount of the emulsion, which makes the preparation, therefore, not only cost-efficient, but also convenient for transportation and storage in practice.
CN103030646A Benzodioxane derivative, and preparation method thereof and application of derivative in medicines The invention relates to a benzodioxane derivative, a preparation method thereof and application of the derivative in medicines. Specifically, the invention relates to a novel benzodioxane derivative shown as a formula (I), medial salt thereof or a medicine composition containing the derivative, and a preparation method of the derivative. The invention further relates to a use of the benzodioxane derivative and the medial salt thereof or the medicine composition containing the derivative in preparing therapeutic agent, especially GPR 40 agonist, and a drug for treating the diseases such as diabetes, metabolic disorders and the like, wherein each substituent group in the formula (I) is as defined in the description.
WO2009014674A1 Heterocyclylamides as gut microsomal triglyceride transport protein inhibitors Compounds represented by formula (I) are inhibitors of gut microsomal triglyceride transfer protein. Such compounds are useful in treating diseases or conditions such as diabetes and obesity, along with patients are risk for developing such diseases or conditions.
CN103479683A North cordyceps sinensis sporophores cultivated in large scale and health care and pharmaceutical application thereof The invention provides north cordyceps sinensis sporophores cultivated in a large scale, the north cordyceps sinensis sporophores comprise 0.3%-3% of north cordyceps sinensis sporophore cordycepin, 8%-30% of cordyceps polysaccharide, 0.055%-0.25% of adenosine and 10%-35% of protein, and according to the large scale cultivation, the contents of effective components in the sporophores can be improved by using a controllable light cultivation rack to regulate and control light intensity and light cycle for light cultivation. The present invention also provides health care products of the north cordyceps sinensis sporophores cultivated in a large scale and the application of the north cordyceps sinensis sporophores cultivated in a large scale in preparation of liver protecting drugs, kidney tonifying drugs, immune cell growth promoting drugs and drugs for enhancing the body's nonspecific resistance.
EP2098533A1 Esters of glucuronide prodrugs of anthracyclines and method of preparation and use in tumor-selective chemotherapy The invention relates to novel esters and in particular to novel water soluble esters of glucuronide prodrugs of anthracyclines their synthesis and use in tumor-selective chemotherapy. It appeared that in the final step in the synthesis of these prodrugs, i.e. the coupling of the glucuronide spacer moiety to the parent drug molecule, protection of the sugar hydroxyls is, surprisingly, no longer required. A process for the preparation of these unprotected sugar spacer moieties is also disclosed.
CN103232490A Nucleoside compounds with HIV-1/HBV viral replication inhibition activity, preparation methods thereof, and antiviral applications thereof The invention discloses acyclic nucleoside compounds with an HIV-1/HBV viral replication inhibition activity, preparation methods thereof, and antiviral applications thereof. The invention also discloses a general formula I of the compounds. R1 is hydrogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C5-6 aryl, or C5-12 aralkyl. R2 is a side chain of any natural or pharmaceutically acceptable amino acid. When the side chain contains carboxyl, the carboxyl is esterified optionally by using alkyl or aryl. The invention also discloses preparation methods of the compounds represented by the structural general formula I and a structural general formula II, and medicine compositions comprising the compounds. As a result of experiments, the compounds provided by the invention have the activity of inhibiting HIV-1/HBV viral replication. One of the compounds has activity higher by more than 385 times that of a current AIDS-treating medicine tenofovir disoproxil fumarate (TDF), and higher fat-solubility than TDF. The compounds can be used in developments of medicines used for treating AIDS or hepatitis B.
CN102603525A Anthraquinone derivative, as well as preparation method and application of anthraquinone derivative serving as antibacterial agent The invention provides an anthraquinone derivative, as well as a preparation method and application of the anthraquinone derivative serving as an antibacterial agent. The preparation method comprises the following steps: culturing a strain of Nigrospora sp. (HM565952) in a strain culture medium; fermenting the nigrospora sp. in a fermentation culture medium; filtering the fermentation broth, removing thallus, and extracting the fermentation broth with ethyl acetate; concentrating the extract, and performing chromatographic separation, and concentrating the eluent to obtain two types of yellow powder, namely 3,5,8-Trihydroxy-7-methoxy-2-methylanthracene-9,10-dione and austrocortirubin; and adding an acetic anhydride reagent in a solution dissolved with the compound, and reacting to obtain the anthraquinone derivative. The anthraquinone derivative obtained from the Nigrospora sp. (HM565952) has selective inhibitory activity to Bacillus subtilis, Bacillus cereus, Micrococcus tetragenus, Micrococcus lutea, Escherichia coli, Staphylococcus aureus, Staphylococcus albus, Vibrio parahaemolyticus and Vibrio anguillarum, and can be used for developing selective bacteriostatic agents; and the raw materials can be produced on a large scale, and not limited by resources. Therefore, the anthraquinone derivative has the advantage of wide application prospect.
CN103356581A Application of Sarcaboside A in preparation of drug for treating liver cancer The invention discloses application of Sarcaboside A in preparation of a drug for treating liver cancer, which belongs to the technical field of new applications of drug. According to the invention, the in-vitro MTT (Methyl Thiazolyl Tetrazolium) antitumor activity evaluation discovers that Sarcaboside A also has an obvious inhibiting effect on the growth of human liver cancer cell strains HepG2, MHCC-LM3, Bel-7402 and HuH-7. Thus, Sarcaboside A can be used for preparing an anti-liver lung cancer drug and has good development and application prospects. The application of Sarcaboside A in preparation of the drug for treating liver cancer is disclosed for the first time. The skeleton type is brand new and Sarcaboside A has unexpectedly high inhibitory activity on liver cancer cell.
CN102526654A Pill for aversion to cold and adiapneustia The invention is used for curing influenza of flu-A, flu-B, plateau cold poison, malaria, plague, aversion to cold, adiapneustia and the like. Gastrodia elata is used for calming liver wind and removing contraction, ephedra is sued for enabling a patient to sweat to remove cold symptom, and realgar and rheum officinale are utilized to kill all plague symptom virus. Cinnabar, liquorice and the like are utilized to calm hearts down, soothe the nerves, purge intense heat, clear summer hot, remove polydipsia, cure dizzy, dyspepsia and fatigue, facilitate defecation and remove drowsiness. Twelve regular channels are unobstructed, accumulation in vital organs is removed, and heat accumulation and poison accumulation are removed by moderating herbs to enable effects to reach nidus to remove plague quickly. Patients such as the old, the young or those who have not been cured for a long time can take one pill or two pills (only for serious patients) to sweat to be cured. All flu plague virus no whether having converted into other diseases or having not converted into other diseases can be cured by the pill. The pill is good in effect, but has poor curing effects on ordinary colds.
EP1819697A1 3-(indolyl)-4-arylmaleimide derivatives and their use as angiogenesis inhibitors The present invention relates to a compound of formula (I) wherein R1 is H, C1-C6-alkyl, phenyl-C1-C4-alkyl or phenyl, R2 is a phenyl group which is substituted with 2 or 3 C1-C6-alkoxy groups and R3 is indolyl or azaindolyl which may carry one or two substituents independently selected from C1-C6-alkyl, C1-C6-alkoxy, phenyl, OH, halogen, NH2, C1-C6-alkylamino, di-C1-C6-alkylamino, heteroaryl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and heterocyclyl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula 1 and of the salts thereof. The compounds of formula (I) are suitable for controlling angiogenesis.
CA2656905A1 Azaindole derivatives with a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition The invention concerns azaindole derivatives having the general formula (I) wherein the symbols have the meanings given in the specification. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.
CN103739654A 28-O-beta-D-glucosyl ursolic acid, and preparation method and application thereof The invention relates to the field of biological medicines, and particularly discloses a 28-O-beta-D-glucosyl ursolic acid (I) and a preparation method thereof by biotransforming ursolic acid by a strain with the collection number of NRRL1086. The invention also discloses application of the 28-O-beta-D-glucosyl ursolic acid in the anti-inflammatory aspect.
CA2703472A1 Methods for treating substance dependence The present invention provides methods for treating alcohol dependence and preventing relapse in subjects in protracted alcohol abstinence. Also provided are methods for treating subjects suffering from cannabis dependence. Typically, these methods entail administering to the subjects in need of treatment a therapeutically effective amount of gabapentin, an analog of gabapentin, or pharmaceutically acceptable salt thereof.
US20080199428 Administering deferasirox, 4-(3,5-Bis-(2-hydroxyphenyl)-(1,2,4)-triazol-1-yl)benzoic acid, interferon and ribavirin; hepatitis and non-alcoholic steatohepatitis The invention relates to the use of 4-[3,5-Bis-(2-hydroxyphenyl)-[1,2,4]-triazol-1-yl]benzoic acid (hereinafter referred to as “Compound I”) for the manufacture of pharmaceutical compositions for the treatment of liver diseases in humans in which iron plays a role in pathogenesis, including viral diseases, such as chronic hepatitis C, optionally in conjunction with antiviral agents and for the treatment of non viral diseases, such as non-alcoholic steatohepatitis and non-alcoholic fatty liver disease.
US7078414 Derivatives of 3-guanidinocarbonyl-1-heteroaryl-pyrrole, preparation process and intermediates of this process, their use as medicaments, and pharmaceutical compositions comprising them The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-pyrrole derivatives of formula (I) wherein R1 to R3 and Ar are as defined herein, pharmaceutical compositions comprising such derivatives, methods of treatment comprising administering such derivatives, and processes for their preparation
WO2006026533A3 Methods of treatment of amyloidosis using ethanol cyclicamine derivatives aspartyl protease inhibitors The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein. The compounds are propanol derivatives substituted by a cyclic amine.
CN1679897A Bioamino acid capsules and preparation thereof A biologic amino acid capsule as a health-care food for protecting human mechanism, improving immunity and delaying senility is prepared from 18 amino acid, white sugar and 5 Chinese-medicinal materials including tuckahoe, astragalus root, tangerine peel, liquorice root, etc.
US20090118373 Inhibition of COX-2 and/or 5-LOX activity by fractions isolated or derived from hops A natural formulation of compounds isolated or derived from hops which inhibit the activity of cyclooxygenase-2 (COX-2) and/or 5-lipoxygenase (5-LOX) is disclosed. The hops formulations may be administered to a mammal to treat or inhibit a pathological condition associated with the activity of COX-2 and/or 5-LOX in such a mammal.
CN1582949A Enteric soluble preparation of Alun phosphorate and its preparing method An enteric allenphosphonate in the form of tablet or capsule is prepared from allenphosphonate, medicinal auxiliary and enteric coating.
US20110313233 Down-regulation of cold shock proteins for cancer treatment The present invention is in the field of treatment of diseased tissues, including cancerous tissues. In one embodiment, the present invention provides methods of identifying tissues that down-regulate cold shock proteins in response to environmental stresses, such as heat. The present invention also provides methods of treatment of diseased tissues comprising down-regulation of cold shock proteins, as well as environmentally stressing (e.g., heating) the tissues, in combination with one or more additional therapies.
CA2736406A1 Compositions comprising diethanolamine salts of trepostinil in the treatment of pulmonary hypertension and other cardiovascular diseases This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have formula (I).
WO2008080986A1 Furan derivatives, method of synthesis and uses thereof The present invention relates to furan derivatives of formula (I), their method of synthesis and uses thereof. Concretely, the compounds disclosed have proved to be inhibitors of glycogen synthase kinase 3β, GSK-3 β, which is known to be involved in different disease and conditions, such as Alzheimer's disease or non-insulin dependent diabetes mellitus. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a GSK-3 mediated disease or condition.
US20100203113 Wnt signalling inhibitors, and methods for making and using them The invention provides dBHD-based compositions and dBHD analog compositions, and pharmaceutical compositions comprising them, e.g., in the form of liposomes and nanoparticles comprising them, and methods of making and using them. In one embodiment, these dBHD analogs are used to inhibit a dysfunctional stem cell and/or a cancer (tumor) stem cell.
CN101658510B Coenzyme Q10 self-emulsifying microcapsules and preparation method thereof The invention discloses coenzyme Q10 self-emulsifying microcapsules, which are characterized in that: the coenzyme Q10 self-emulsifying microcapsules are prepared from the following raw materials: coenzyme Q10, lipid, a surfactant and a wall material of which the weight ratio is 1-20:5-30:5-30:30-90; and the preparation method comprises the following steps: respectively taking the coenzyme Q10, the lipid and the surfactant, putting into a material mixing tank provided with a stirrer device, and stirring and mixing evenly; adding water 5 to 20 times of the mixture, and stirring to form homogeneous solution; and adding the wall material, stirring to dissolve the wall material, and performing spray drying to prepare the coenzyme Q10 self-emulsifying microcapsules. The coenzyme Q10 self-emulsifying microcapsules are a self-emulsifying solid preparation; and a coenzyme Q10 self-emulsifying composition is coated in the microcapsules to improve the stability of the coenzyme Q10 self-emulsifying preparation, and the coenzyme Q10 self-emulsifying preparation can be automatically emulsified into micro emulsion in gastric juice, increases the absorption of the coenzyme Q10, improves medicinal effect, and has good treatment effect on diseases such as cardiovascular disease, hepatitis, low immunity and the like.
CN101845075A 6-substituted-4-azepine-A-homo-3-oxosteroid compound and application thereof to preparing anti-tumor medicine The invention discloses a 6-substituted-4- azepine-A-homo-3-oxosteroid compound, which has a chemical structural formula as shown as in a formula I, wherein X is OH, =NOH, OSO3Na, =O, =NNH2, =NCSNH2, =NCONH2, =NCNHNH2, =NNHCSNH2, =NNHCONH2, OCH2CH2N(R')2, N(CH2CH2Cl)2, halogen, =S, SH and OR'; R' is a common alkyl group, a linear chain with 1-14 C atoms or a carbon chain substituting branched achains at different positions or a carbon chain with different functional group substituted groups, or functional groups containing different heteroatoms such as OH, =NOH, OSO3Na, =O, =NNH2, =NCSNH2, =NCONH2, =NCNHNH2, =NNHCSNH2, =NNHCONH2, OCH2CH2N(R')2, N(CH2CH2Cl)2, halogen, =S, SH and OR'. The experiment shows that the 6-substituted-4- azepine-A-homo-3-oxosteroid compound has remarkable inhibition action on a plurality of tumor cells and can be used for preparing a medicine for treating cancer.
CN103301076A Alprostadil frozen-drying lipid emulsion and preparation method thereof The invention provides an alprostadil frozen-drying lipid emulsion and a preparation method thereof. The emulsion comprises the following compositions in percentage by mass: 0.0005-0.01% of alprostadil, 1-10% of oil for injection, 0.01-5% of an emulsifier, 0.02-2% of a stabilizer, 0-0.5% of an antioxidant, 1-20% of a freeze-drying protecting agent, and proper pH regulator and water for injection; the preparation method comprises the steps of: stirring alprostadil and oil for injection, and evenly mixing to obtain an oil phase; stirring freeze-drying protecting agent and water for injection to obtain a water phase; respectively the emulsifier, antioxidant and stabilizer into the water phase or the oil phase according to the solubility; mixing the water phase and the oil phase, carrying out high-speed stirring and dispersion, carrying out constant volume on the water for injection, regulating the pH value to obtain initial emulsion; transferring the initial emulsion into a high-pressure homogenizer for homogenizing for many times, then filtering, subpackaging, freeze-drying to obtain the alprostadil frozen-drying lipid emulsion. The alprostadil frozen-drying lipid emulsion is more stable and more uniform, the preparation technology and method can be simplified, and the economic efficiency can be improved.
WO2013184902A1 Chemical transformations of (-)-codeine to afford derivatives of codeine and morphine thereof The present invention relates to methods for the synthesis of morphine, codeine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency, steroselectivity, and overall yield of said codeine and morphine related derivatives and intermediates thereof. The present invention relates to new codeine and morphine related derivative compositions.
US20110052599 Facilitation of Oocyte, Zygote and Pre-Implantation Embryo Maturation Compositions and methods are provided for enhancing the survival and promoting the maturation of mammalian oocytes, zygotes and preimplantation embryos. BDNF or BDNF agonists may be administered to an individual, or to cells in vitro, to enhance cellular maturation, embryo growth and fertilization. Accordingly, compositions comprising BDNF are herein presented for use in promoting in vivo oocyte maturation as well as for use as a component in culture media for promoting preimplantation maturation of zygotes and embryos, for instance, for use with in vitro fertilization procedures and for the production of stem cells. Additionally, compounds that interfere with the binding of BDNF to its receptor may be administered to an individual to prevent oocyte maturation, thereby acting as a contraceptive. The BNDF receptor, TrkB, and BDNF also find use in the screening and design of agonists and antagonists for use in the methods of the invention.
WO2013147899A1 Osteoprotegerin derived composition and use thereof A therapeutic composition is described that can be used for treating or prevention of diseases association with bone resorption, particularly of a metastatic carcinoma. In certain aspects, the composition is based on a polypeptide which includes the leading 215 amino acids of the human osteoprotegerin followed by the Fc portion of the human IgGl protein. DNA expression vectors and expression systems for overproducing the polypeptide in mammalian cells are also provided for.
WO2008115140A1 Quinoline derivatives, pharmaceutical compositions comprising them, and their use in treating central nervous system and peripheral diseases Compounds of Formula (I) wherein R1, R2, n and R3 are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
US20050063940 Use of (poly)ethoxylated fatty acid glycerides for enhancing bioadhesion of a liquid pharmaceutical applied to a mucous membrane; use delivering active agents to plants, fish gills One or more mono- or diglycerides according to formula I: wherein R1, R2, and R3 are selected from the group consisting of from C6 to C26 fatty acids, PEG polymers and hydrogen, provided that at least one of R1, R2 and R3 is a C6-C26 fatty acid residue and at least one of R1, R2 and R3 is a PEG polymer residue for use as a bioadhesive agent for medical purposes. The agent may be used in the delivery of e.g. protein, peptides or antigens over mucosal membranes.
US7618619 For use in ocular surgery; containing a vital dyes, especially a disazo dye, that does not diffuse out of the visco-elastic composition. The invention relates to a visco-elastic composition for use in ocular surgery and to a method of using said composition. Specifically, the present visco-elastic composition comprises a visco-elastic substance and at least one vital dye. The invention enables a visual distinction of the visco-elastic composition from the surrounding aqueous or intraocular structures during ocular surgery, so that the amount present within the eye, the location and the effects of the visco-elastic material can be better monitored.
US7531635 Monoclonal antibodies or functional fragment; immunoassay kit; female fertility diagnosis; Premature ovarian failure Disclosed herein are novel nucleic acid and protein sequences that are essential to fertility. In particular, human Mater cDNA and protein sequences are provided. Functional MATER is required for female fertility; zygotes that arise from Mater null oocytes do not progress beyond the two-cell stage. MATER-protein specific binding agents, such as antibodies, are described. Methods are described for detecting MATER protein in a subject, including methods for determining whether a subject has a biological condition associated with abnormal Mater expression. Also provided are kits for detecting MATER protein in a subject.
WO2007101873A2 Betulonic acid esters and betulinic acid polyalkylene-glycol derivatives for the treatment of viral infection and cancer The present invention relates to betulonic and betulinic acid derivatives and, in particular, to C-28 and C-3 derivatives. The present invention relates to betulonic acid esters, dihydro-betulonic acid esters, PAG-modified betulinic acid derivatives, and PAG-modified dihydro-betulinic acid derivatives. Betulinic acid and derivatives thereof may be bound to a poly(alkylene glycol) (PAG) such as poly(ethylene glycol). Binding may be via a linker, such as a diamine, an amino acid, a peptide, an ester or a carbonate. The compounds of the present invention may be used for the treatment of cancer or a viral infection. The present invention also provides pharmaceutical compositions comprising the compounds of the present invention. The present invention further provides processes for the preparation of the compounds of the present invention, for example, from betulin.
EP2699539A2 Cyclopropyl derivatives and methods of use The disclosure relates to cyclopropyl derivatives and methods of use. In some embodiments, the disclosure relates to methods of managing medical disorders with pharmaceutical compositions disclosed herein administered to subject in need thereof. In certain embodiments, the disclosure relates to methods of managing mental disorders, mood disorders, pain, and fibromyalgia and related conditions with pharmaceutical compositions disclosed herein.
CN101940577A Compound-type aqueous multiple-effect environmentally-friendly bactericide as well as preparation method and applications thereof The invention relates to a compound-type aqueous multiple-effect environmentally-friendly bactericide as well as a preparation method and applications thereof. The bactericide is mainly composed of the following components in parts by weight: 5-15 parts of chlorhexidine acetate, 1-15 parts of polyethylene glycol octyl phenyl ether, 0.1-3 parts of sulfacetamide sodium and 52-94.4 parts of purified water or distilled water. The preparation method comprises the steps of mixing and heating. The compound-type aqueous multiple-effect environmentally-friendly bactericide is applied in human bodies, livestock skins, mucosas and substance surfaces for sterilizing, and has the effects of diminishing inflammation, converging, relieving pain, relieving itch and removing peculiar smell. Compared with the prior art, the bactericide of the invention has the advantages of more sterilization categories, high sterilization rate, simple manufacturing process, low cost, wide application range, more application objects, accurate curative effect position and reliable safe use accordance.
EP1590333A1 Glycogen synthase kinase 3beta inhibitor, composition and process for the preparation thereof Novel compounds having hydroxybenzoimidazole carboxylic amide are useful for inhibiting glycogen synthase kinase 3β (GSK-3β).
WO2010098261A1 Risperidone-containing transdermal preparation and adhesive patch using same Disclosed is a transdermal preparation which contains risperidone and/or a pharmaceutically acceptable salt thereof as a medicine. The transdermal preparation contains 1-20 parts by mass of the medicine relative to 100 parts by mass of the total of the preparation, while having a skin permeation rate of 0.5-30 µg/cm2/hour and a drug diffusion coefficient in the skin of from 1.2 × 10-6 cm/hour to 10.0 × 10-6 cm/hour.
WO2012134446A1 Epiandrosterone and/or androsterone derivatives and method of use thereof Disclosed herein are epiandrosterone and androsterone derivatives of Formula (II), process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
CN101829044A Tamibarotene solid preparation and preparation method thereof The invention discloses a tamibarotene solid preparation, which comprises tamibarotene, disintegrant, filler and lubricant. The tamibarotene solid preparation is characterized in that over 70 percent of the tamibarotene solid preparation can be dissolved in 20 minutes. Formula study experiments prove that the tamibarotene solid preparation comprises 2 to 3 weight percent of tamibarotene, 5 to 7 weight percent of disintegrant, 90 to 92 weight percent of filler and 0.5 to 0.7 weight percent of lubricant. Preferably, the tamibarotene solid preparation comprises 2.3 weight percent of tamibarotene, 5.8 weight percent of disintegrant, 91.2 weight percent of filler and 0.6 weight percent of lubricant.
WO2014134306A1 Heterocyclic inhibitors of the sodium channel The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (l)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotrophic lateral sclerosis, glaucoma, ischemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.
CN1771950A Freeze dried nimodipine composition and its prepn The present invention discloses one kind of freeze dried nimodipine composition and its preparation. The freeze dried nimodipine composition consists of nimodipine, surfactant, polyglycol as solvent, excipient glycerin and mannitol, etc. The freeze dried nimodipine composition has simple preparation process, high bioavailability, excellent dissolubility and stability, and easy preservation.
CN101948488A Ruthenium-selenium coordination compound and application thereof in preparing fluorescent probe and antineoplastic medicine The invention discloses a ruthenium-selenium coordination compound and a synthesis method and an application thereof. The molecular formula of the coordination compound of the invention is [Ru (phen) 2p-MOPIP] 2+, the chemical name of the coordination compound is 2-phenanthroline-1, 10-phenanthroline diazole ruthenium coordination compound, the structure of the coordination compound is shown as the general formula (I). The ruthenium-selenium coordination compound of the invention can be served as the fluorescent probe for identifying tumour cells and the receptor on a cell membrane, and can enter the cytoplasm and finally be enriched in the cell nucleus region. As the fluorescent probe, the ruthenium-selenium coordination compound of the invention react with the cancer cell for 30min, then fluorescence intensity remarkably increases, and with the extension of time, the fluorescence intensity further increases; however, the coordination compound shows weak fluorescence or no fluorescence in normal cells. Therefore, the ruthenium-selenium coordination compound of the invention can be used for detecting tumour cells and carrying out fluorescence imaging on the living body and can be also used for preparing medicines for preventing or treating cancers.
CN102895252A Application of Houttuynoid A in drugs for treating lung cancer The invention discloses an application of Houttuynoid A in preparing drugs for treating lung cancer. As a compound, the Houttuynoid A shows high anti-lung cancer activity, can be used for preparing the anti-lung cancer drugs and belongs to the technical field of new uses of the drugs. The Houttuynoid A is capable of remarkably inhibiting non-small cell lung cancer cells A549, large cell lung cancer cells NCI-H460, lung squamous cancer cells HTB-8 and human lung epidermoid carcinoma cells QG-5, but is smaller in effect of inhibiting human normal hepatocytes LO2 and peripheral blood lymphocytes, i.e. obvious selectivity is shown. The application of the Houttuynoid A in preparing the drugs for treating the lung cancer is disclosed for the first time. Moreover, the skeleton type of the Houttuynoid A is fire-new, and how strong the inhibitory activity of the Houttuynoid A on the lung cancer cells is unexpected.
US20110082118 Onychomycosis Treatment Delivery System A topical treatment for onychomycosis and Tinea pedis comprising a delivery system further comprising at least one hydroxy acid agent having a pH-pKa value of 0.5 or greater and at least one antifungal agent formulated into creams, lotions, gels, sprays, foams, pads, films, patches, and solutions.
CN101947311A Plasma substitute combination The invention relates to a plasma substitute combination which is prepared by crosslinking product polymerized polypeptide of beef bone or pig bone gelatine with a weight-average molecular weight of 27500-39500, sodium hydroxide, sodium chloride, potassium chloride, calcium chloride, L-Lysine Hydrochloride and water for injection according to the proportion by weight of 3-5:0.3-0.5:3.6-3.9:0.08-0.12:0.05-0.06:1.5-2.0:480-500. Osmotic pressure, glutinousness, pH value and electrolyte of the plasma substitute combination of the invention are all similar to those of human plasma; in addition, the plasma substitute combination is provided with a similar spherical molecular structure similar to the spherical molecular structure of human albumin and volume effect equivalent to the volume effect of the human albumin, can maintain balance between endovascular fluid and interstitial fluid, does not lead to tissue dehydration and pulmonary edema and has the function of maintaining blood volume and elevating blood pressure. In addition, clinically applied, the plasma substitute combination has the advantages not found in human blood, for instance, blood type matching is not needed when blood transfusion is carried out, cross infection of hepatitis, AIDS and other diseases caused by blood transfusion can be avoided, so that the plasma substitute combination is suitable for clinical emergency treatment. Moreover, the plasma substitute combination of the invention features low sensitization, small side effect as the plasma substitute and good safety.
CN103463368A Aerosol used for treating traumatic injury and preparation method thereof The invention discloses an aerosol used for treating traumatic injury and a preparation method thereof. The aerosol is prepared from Gaultheria yunnanensis, Laportea sinensis, Asiatic toddalia root, pink reineckea herb, creeping oxalis, longleaf luckyweed flower, borneol, camphor and accessories. The aerosol is capable of promoting blood circulation to remove blood stasis and relieving swelling and pain. According to the invention, pure Miao medicines are used as raw materials to prepare the aerosol, and the aerosol has the advantages of long action time, convenient usage, a good curative effect and easy storage; a film forming material is added, a propellent is employed to spray the aerosol onto an affected part to form a medicinal film, so external infection is avoided and the aerosol is a sustained release preparation and especially applicable to the majority of patients.
WO2008001499A1 Prophylactic and/or therapeutic agent for rheumatoid arthritis Disclosed is an agent having excellent therapeutic and prophylactic effects on rheumatoid arthritis. Specifically, disclosed is a prophylactic and/or therapeutic agent for rheumatoid arthritis, which comprises a combination of 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]- 2H-pyridazin-3-one and an HMG-CoA reductase inhibitor.
WO2007088712A1 Neuronal cell death inhibitor and screening method [PROBLEMS] To provide an agent for inhibiting or avoiding the neuronal cell death caused by glutamic acid. [MEANS FOR SOLVING PROBLEMS] Disclosed is a neuronal cell death inhibitor comprising a compound having an inhibitory activity on the production and/or release of glutamic acid in a microglia. By inhibiting the production and/or release in a microglia, neurite bead-like degeneration or neuronal cell death can be inhibited.
WO2013057469A1 Pharmaceutical antiretroviral compositions The present invention relates to pharmaceutical antiretroviral compositions comprising a combination of antiretroviral agents, the manufacturing process thereof, and use of the said compositions for the prevention, treatment or prophylaxis of diseases caused by retroviruses, especially acquired immune deficiency syndrome or an. HIV infection.
EP1909816B1 Cnf1 bacterial toxin protein from e. coli as analgesic The invention concerns new uses in medical field of the dermonecrotizing protein factors of bacterial origin, particularly from Escherichia coli and related uses in medical field.
US20090110718 Derivatives of tiacumicin B as anti-cancer agents New derivatives of tiacumicin B are disclosed and are presented by the general formula: wherein R is The use of these derivatives as a method for treating cancer or tumor is disclosed. A method of treating cancer or tumor by administrating the patient a composition comprising a therapeutically effective amount of the tiacumicin B is also disclosed.
CN103623160A Patch for promoting blood circulation to remove meridian obstruction and eliminating cold to stop pain and preparation method thereof The invention discloses a patch for promoting blood circulation to remove meridian obstruction and eliminating cold to stop pain. The patch consists of a formula A, a formula B, a formula C, a formula D, a formula E, and a formula F, wherein the formula A is prepared from the following medicinal materials in parts by weight: 15-40 parts of magnetite, 10-30 parts of unprocessed radix aconiti, 10-30 parts of radix aconite, 10-30 parts of raw arisaema heterophyllum blume, 10-30 parts of unprocessed pinellia ternate, 5-15 parts of asarum, 5-15 parts of small cassia nomame, 10-30 parts of jasmine, 5-30 parts of frankincense, 5-30 parts of myrrh, and 5-30 parts of scorpio; the formula B is prepared from the following medicinal materials in parts by weight: 20-40 parts of semen momordicae, 20-40 parts of semen strychni and 40-80 parts of semen brassicae; the formula C is prepared from the following medicinal materials in parts by weight: 10-30 parts of camphor and 10-30 parts of borneol; the formula D is prepared from the following medicinal material in parts by weight: 150-300 parts of sesame oil; the formula E is prepared from the following medicinal material in parts by weight: 20-50 parts of chlordiazepoxide ketone.
US7417043 3-substituted 4-(phenyl-N-alkyl)-piperazine derivatives; central nervous system disorders; dualistic dopaminergic action profile with antagonist-like effects on brain neurochemistry and mild agonist-like effects on normal behavior, induce inhibition of behavior in hyperactivity; oral bioavailability A 3-substituted 4-(phenyl-N-alkyl)-piperazine compound of the following formula: wherein R1 is selected from the group consisting of OSO2CF3, OSO2CH3, SO2R3, COCF3, COCH3 and COCH2CH3, wherein R3 is as defined hereafter; R2 is selected from the group consisting of C1-C4 alkyls, allyl, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl and 4,4,4-trifluorobutyl; R3 is selected from the group consisting of C1-C3 alkyls, CF3, and N(CH3)2; with the proviso that when R1 is SO2R3 and R3 is a C1-C3 alkyl, then R2 is not CH2CH2OCH3; or a pharmaceutically acceptable salt thereof are provided. Also, pharmaceutical compositions comprising the above compound and methods wherein the above compound is used for the treatment of various disorders are provided.
CN101966195A Application of quercetin in preparing medicaments for treating organ transplant rejection reactions The invention discloses the application of quercetin in preparing medicaments for treating organ transplant rejection reactions. The quercetin can be used for treating rejection reactions generated by inhibited tissue organs, such as liver, kidney, bone marrow, cornea, skin and heart transplantation. The invention also relates to the preparation of quercetin compositions.
US20070299088 Novel Uses of 2-Phenyl-Substituted Imidazotriazinone Derivatives The invention relates to the use of PDE 5 inhibitors, and especially of known 2-phenyl-substituted imidazotriazinone derivatives for producing medicaments for the treatment of symptoms that can be treated by increasing cGMP levels in certain tissues, such as acute myocardial infarction and damage caused by reperfusion, various symptoms in the female and male reproductive system and urogenital tract, gastrointestinal diseases, damage caused by diabetes, and liver failure.
WO2013057208A1 Compositions and methods for reducing the proliferation and viability of microbial agents The disclosure relates to formulations of an antimicrobial agent, a lipid, and optionally a surfactant, and uses thereof for reducing the proliferation and viability of microbial agents. In certain embodiments the disclosure relates to a single composition that includes two antimicrobial agents and method of using such single compostions.
US20100113492 Substituted Aminopyrimidines as Cholecystokinin-1 Receptor Modulators Certain novel substituted aminopyrimidines are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.
WO2008020045A1 Tetrahydrobenzothiophene derivatives Compounds of a certain formula I, in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.
CN102048884A Weight-losing composition containing guarana extract The invention provides a weight-losing composition which comprises L-carnitine or a pharmaceutically acceptable salt of the L-carnitine and a guarana extract, and the invention simultaneously provides a formulation of the weight-losing composition and a preparation method thereof. The weight-losing composition can accelerate the burning of fat in a human body, and effectively oxidize, decompose and convert the fat in the human body to energy, thereby achieving the purpose of naturally controlling and reducing the body weight.
CN103392874A Food-grade health tea soluble granules capable of nourishing kidney The invention discloses food-grade health tea soluble granules capable of nourishing kidney, and belongs to the field of nutritious food. Effects are excellent, and efficacy is quick. The food-grade health tea soluble granules comprise raw materials such as American ginseng, Chinese angelica, motherwort, polyporus and theanine; is capable of reinforcing the vital energy and consolidating the constitution, reinforcing Qi and nourishing blood, and promoting blood circulation and removing blood stasis; and has advantages of excellent effects and quick efficacy.
US7407974 e.g. 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide}; anticoagulant, thrombolytic agent; thrombus formation within blood vessels; cardiovascular disease The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.
CN102911290A Method for separating and purifying heparin sodium and heparan sulfate from heparin byproducts The invention discloses a method for separating and purifying heparin sodium and heparan sulfate from heparin byproducts. The method comprises the steps of dissolving raw heparin byproducts, adding potassium acetate to precipitate and separate heparin sodium, adding potassium acetate to precipitate heparin sodium after precipitating and dissolving heparin sodium, collecting a precipitate, dissolving and then conducting fractional precipitation repeatedly with anhydrous alcohol to prepare the heparin sodium with a higher purity, adding a benedict reagent and a saturated sodium hydroxide solution to supernate, centrifuging to obtain a solution containing the heparan sulfate, removing copper ions with a decoppering agent, adding active carbon to absorb the precipitate, decolorizing and filtering, and then absorbing and eluting with anion exchange resin to obtain the high-purity heparan sulfate by separation. According to the method, the high-purity heparin sodium and heparan sulfate can be separated again from the byproducts used for producing the heparin sodium, so that financial resources and material resources required for storing or discarding a large number of heparin byproducts can be saved, wastes can be changed into valuables, the byproducts are recycled, the cost is saved greatly, and a value is created.
WO2013176223A1 Pharmaceutical composition for treating inflammatory disease Provided is a pharmaceutical composition comprising a liposome that encapsulates an immunosuppressant such as FK506, FTY720, or cyclosporine A as the active ingredient, which is effective in the treatment of inflammatory disease of the circulatory system such as myocardial infarction, myocarditis, or vasculitis syndrome and with which potentiation of activity at a smaller dose than with the immunosuppressant alone and a reduction in side effects are possible.
US20050054735 6-Methoxy-2-naphthylacetic acid prodrugs The present invention provides therapeutically effective amounts of 6MNA prodrugs. The pharmaceutical composition comprises wherein R is H or COR′, wherein R′ is selected from the group consisting of C1 to C6 alkyl, (CH2)m O(CH2)n, (CH2)m(OC2H4)p O(CH2)n, (CH2)m(OC2H4)p, (OCH2H4)p ONO2 and (OCH2H4)p O(CH2)n wherein m is an integer from 2 to 4, and n and p are integers from 1 to 4. Alternatively, R is a therapeutic moiety.
EP1458364B1 Pharmaceutical compositions comprising metformine and glibenclamide for the treatment of type-ii diabetes mellitus Orally administrable pharmaceutical compositions in the form of tablets, comprising glibenclamide and metformin, or pharmaceutically acceptable salts thereof, as active ingredients, maintained separate from one another within the same composition, are described for the treatment of type-II diabetes mellitus.
CN103405468A Use of low-molecular weight oligomannuronate in preparation of drug or health care product for preventing or treating Parkinson's disease The invention provides a use of low-molecular weight oligomannuronate in preparation of a drug or a health care product for preventing or treating Parkinson's disease. According to the invention, marine acidic polysaccharose as a raw material is prepared into a water-soluble low-molecular weight mannuronic acid compound. An experiment proves that the low-molecular weight mannuronic acid can be used for preventing and treating or improving Parkinson's disease, has obvious pharmacological effects and no toxic or side effects on nerve cells and can be taken for a long time. The low-molecular weight mannuronic acid is a marine natural product, has the advantages of rich resources, easy industrialization, high safety, unique structure and good oral absorption, and has a wide market application prospect in prevention and treatment of Parkinson's disease.
EP1758587B1 Use of a pharmaceutical composition comprising calcitriol and clobetasol propionate for the treatment of psoriasis The invention relates to a pharmaceutical composition which is intended for the treatment of psoriasis and which is characterised in that it comprises clobetasol propionate and calcitriol in quantities suitable for once-daily application on the part(s) of the skin affected by psoriasis.
CN103301062A Medium and long-chain lipid emulsion injection preparation method The invention discloses a medium and long-chain lipid emulsion injection preparation method. The method comprises the following steps of: feeding, primary emulsion preparing, homogenizing, filtering, filling, plugging, capping, sterilizing, clarity inspecting, packaging, inspecting and storing. The method is simple in operation process, and a medium and long-chain lipid emulsion injection product can have uniform emulsion granules, various qualified indexes and layering appearance through controlling parameters such as homogenizing pressure and time and the like, so that the preparation stability within 2-3 years can be solved.
WO2013101713A1 A nutritional approach to the use of ergothioneine and vitamin d2 for hair, nail and skin growth Nutritional products, including food and/or beverage compositions, pharmaceutical and cosmetic preparations and methods of use are disclosed for the prevention, suppression and treatment of skin, hair, and nail conditions for the improvement of skin, hair and nail growth through the identification and/or use of stem cells, as well as maintenance of healthy tissues. Uses of Ergothioneine and/or Vitamin D to neutralize free radicals, and improve skin, hair and nail growth are disclosed.
US20080227737 Comprises nucleotide sequences for use as diagnostic tools in identifying allelic sequences associated with blood sugar defects Methods and compositions related to novel genes associated with type 2 diabetes mellitus.
US20100068214 Identification of Candidate Vaccine Antigens from Dichelobacter Nodosus This invention relates to a prophylactic and/or therapeutic treatment of footrot, and in particular to a vaccine effective in prophylactic and/or therapeutic treatment of footrot. Specific polypeptides of Dichelobacter nodosus have been identified as vaccine candidates. In some embodiments the polypeptide is expressed more strongly when the bacterium is grown in vivo or is expressed more strongly in the presence of ovine hoof powder. In other embodiments the polypeptide are reactive against sera recovered from animals repeatedly infected with D. nodosus.
US7105560 Use of etodolac in the treatment of multiple myeloma A method of treating multiple myeloma (MM) is provided comprising administering an amount of etodolac to a subject afflicted with MM that is effective to selectively reduce the viability of and/or to sensitize the cancer cells to an anti-cancer agent.
WO2012107262A1 Dihydrobenzopyran, thiochroman, tetrahydroquinoleine and tetrahydronaphtalene derivatives and their use in anticancer therapy New dihydrobenzopyran, thiochroman, tetrahydroquinoleine and tetrahydronaphthalene derivatives and their use in anti-cancer therapy with the general formula (I).
EP1096975B1 Use of a3 adenosine receptor antagonists in the manufacture of a medicament for reducing intraocular pressure A method for decreasing intraocular pressure by administering an A3 subtype adenosine receptor antagonist, a calmodulin antagonist or an antiestrogen such as tamoxifen. These agents, by inhibiting influx or promoting efflux of aqueous humor, can be used to treat glaucoma.
CN103393609A Dexrazoxane-containing composition and preparation method thereof, and dexrazoxane freeze-drying preparation and redissolving solvent thereof The invention relates to the field of medicine, in particular relates to the fields of preparation and application of dexrazoxane, and more particularly relates to a dexrazoxane-containing composition and a preparation method thereof, and a dexrazoxane freeze-drying preparation and a redissolving solvent thereof. The dexrazoxane-containing composition is a solution consisting of dexrazoxane, hydrochloric acid, water and tertiary butanol, wherein the dexrazoxane concentration of the composition is 20 to 30 mg/mL. The dexrazoxane freeze-drying preparation provided by the invention has excellent stability and the preparation method is easy to industrialize.
US20110165235 Directly pressed aliskiren tablets The invention relates to pharmaceutical compositions which contain the active agent Aliskiren and are suitable for the production of tablets by dry pressing, so that prior wet granulation can be obviated. The invention also relates to tablets which can be obtained by dry pressing of these pharmaceutical compositions and to a method for producing these tablets. The invention furthermore relates to the use of the novel pharmaceutical compositions and tablets for treating hypertension and illnesses associated therewith.
US20110052661 Pet dental hygiene product An edible product for oral hygiene of a pet, the product being chewable by the pet to remove plaque, tartar and stain from the teeth of the pet and to reduce breath odor of the pet. The dental hygiene product includes a body formed of a first set of constituent components and a second set of constituent components, the first set of constituent components including abrasive components and one or more breath freshening components, the combination when chewed by the pet effecting the removal of plaque, tartar and stain and the inhibition of breath odor, the second set of constituent components including an abrasive component and one or more active components, the abrasive component when chewed by the pet effecting the removal of plaque, tartar and stain from the teeth of the pet, the one or more active components being characterized by the active components disrupting growth of bacteria in the pet's mouth thereby inhibiting plaque and tartar formation and breath odor from a bacterial source.
CN101264104A Calf serum de-protein injection and producing method thereof The invention discloses a free protein serum of cow injection and the production method, which is characterized in that: 1). Protein is removed from calf serum before rough filtration is made, thereby collecting the filtrate; 2). The filtrate is extracted using toluene, ethyl acetate and normal butyl alcohol in turn; organic phase is thrown away and water phase is kept for each extraction; 3). Chromatography is made upon the water phase through adopting BIO-GEL-P2 gel, thereby getting free protein serum of cow injection. Active ingredient of the free protein serum of cow injection is polysaccharide. Content of the polysaccharide is 1.0 to 1.2mg/ml and preferred content is 1.17mg/ml.
US20110061649 Device and method for treating respiratory and other diseases A method and device to prevent and cure body diseases caused by infection factors such as: bacteria, virus, fungi, parasites as well as preventing fat accumulation in body blood vessels, lowering blood pressure, lowering cholesterol level in the blood and destroying body organs cancer cells is done by inhaling vapors of fresh crushed or sliced garlic or vapors of synthetic allicin.
EP1451144B1 Compositions for treating acne comprising phytandiol amine The present invention relates to a phytandiol amine derivative represented by the following formula (I) and compositions for treating acne comprising the same: (I) wherein each of Y and Z is OH with the proviso that X is NH2, each of X and Z is OH with the proviso that Y is NH2, and each of X and Y is OH with the proviso that Z is NH2.
EP1596862B1 Use of palonosetron for treating post-operative nausea and vomiting Methods are provided to treat post-operative nausea and vomiting, as well as emesis generally, with 5-HT3 receptor antagonists. In particular, the invention discloses methods for reducing post-operative nausea and vomiting and other emetic events with palonosetron.
US20100240626 Antiemetic-oral contraceptive combination The present invention relates to a method of reducing the incidence of nausea and vomiting associated with the administration of oral contraceptive formulation and a method of preparation of oral contraceptive formulation comprising progestin and/or estrogen and an antiemetic. The preferred oral contraceptive formulation comprises of levonorgestrel and an antiemetic.
US20110207827 Method for determining sensitivity or resistance to compounds that activate the brain serotonin system The invention relates to a method for determining whether a patient suffering from a condition that is susceptible to treatment with a compound that activates the brain serotonin system is susceptible or resistant to treatment with the compound. The method includes establishing whether the patient is a pre-adult, a transition age patient, or an adult and observing whether the genome of the patient contains at least one copy of a BDNF allele having a genetic alteration. The method further includes correlating the presence of the allele containing the genetic alteration with susceptibility or resistance of the patient to the treatment with the compound, wherein a pre-adult patient containing the genetic alteration is correlated as being susceptible to the treatment; a transition age patient containing the genetic alteration is correlated as being susceptible or resistant to the treatment; and an adult patient containing the genetic alteration is correlated as being resistant to the treatment.
US20110305778 Chemically Stabilized Anti-Dandruff Compositions For Use In Personal Care Compositions The present invention is directed to a stabilized anti-dandruff composition comprising about 10 wt. % to about 40 wt. % of an insoluble anti-dandruff agent, about 6 wt. % to about 12 wt. % of a stabilizer, less than about 1 wt. % of a preservative, and about 0.5 wt. % to about 1 wt. % of a neutralizer, and water. In an embodiment of the present invention, it is directed to a stabilized anti-dandruff composition comprising about 10 wt. % to about 25 wt. % of a zinc-containing layered material, about 6 wt. % to about 12 wt. % of a stabilizer, less than about 1 wt. % of a preservative, and about 0.5 wt. % to about 1 wt. % of a neutralizer, and water.
CN102743393A Medicinal composition containing abiraterone acetate and preparation technology thereof The invention belongs to the technical field of medicine, and particularly relates to a medicinal composition containing abiraterone acetate and a preparation technology of the medicinal composition. The medicinal composition comprises abiraterone acetate, a solubilizer, a binder and a disintegrating agent and can be prepared into tablets, granules or capsules. The invention is characterized in that the abiraterone acetate and hydrophilic auxiliary materials are crushed based on a proportion, and the dissolution rate and bioavailability of the medicine are effectively improved, the medicinal composition can be used for treating the prostate cancer.
WO2006027628A2 Naphthalimide derivatives as antiviral agents The present invention relates to the use of naphthalimide compounds of formula (I), wherein A, B, R1, R2, n and Ra are defined herein, and pharmaceutically acceptable salts thereof, for the treatment or prevention of infection by hepatitis C virus.
WO2009152228A9 Use of the combination of phy906 and a tyrosine kinase inhibitor as a cancer treatment regimen This invention provides herbal compositions useful for increasing the therapeutic index of chemotherapeutic compounds. This invention also provides methods useful for improving the quality of life of an individual undergoing chemotherapy. Furthermore, this invention improves the treatment of cancer by administering the herbal composition PHY906 in combination with one or more chemotherapeutic compounds to a mammal undergoing such chemotherapy.
US8343998 Triazolothiadiazole inhibitor of c-Met protein kinase The present invention relates to compound 1, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising Compound 1 and methods of using the compositions in the treatment of proliferative disorders.
WO2006074919A3 3-AMINO-6-ARYL(OR 6-HETEROARYL)-THIENO[2,3-B]PYRIDIN-2-CARBOXAMIDES, PHARMACEUTICAL PREPARATIONS CONTAINING THE SAME AND THEIR USE AS TNFα INHIBITORS The invention relates to the novel 3-amino-6-aryl-thieno[2,3-b]pyridin-2-carboxamides of general formula (1), to methods for producing them, to pharmaceutical preparations containing said compounds and/or the tautomers and optionally the physiologically acceptable salts obtained therefrom and/or the solvates thereof. The invention also relates to the use of said compounds, their tautomers, salts or solvates as inhibitors of TNFα release.
WO2008047224A1 Pyrazolyl-4-oxy-benzonitrile derivatives useful in treating endometriosis Compounds of Formula (I): and pharmaceutically acceptable salts, solvates (including hydrates) of said compounds and salts, or prodrugs of said compound, or pharmaceutically acceptable salts or solvates of said prodrugs, wherein the substituents are as herein defined, may be useful in therapy, for example they may be useful for treating progesterone-mediated conditions such as endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
US20100247663 Microspheres The invention relates to the production of microspheres having radial pores using thermally induced phase separation, especially microspheres for use in tissue engineering.
CN103405460A Therapeutic agent for meniere The invention discloses a therapeutic agent for meniere. The therapeutic agent is mainly prepared from the following ingredients: deanxit, amitriptyline, clonazepam, bayaspirin and perenan. The target spot of the therapeutic agent acts on a plurality of etiological factors of the meniere, so that the therapeutic agent has obvious effects on adjustment of central neurotransmitter, adjustment of autonomic nervous function, improvement of inner ear microcirculation, alleviation of hydrolabyrinth, alleviation of inner ear vascular stricture or occlusion and the like, obviously improves the symptoms such as dizziness, deafness and tinnitus of patients and has no obvious drug side effects.
CA2690293C Methods for determining whether a compound is capable of inhibiting the interaction of a peptide with rage The present invention provides a method for determining whether a compound is capable of inhibiting the interaction of a peptide with a receptor for advanced glycation end product (RAGE), which comprises: (a) admixing: (i) the peptide, wherein amino groups of the peptide are inactivated by derivitization, (ii) RAGE or a fragment thereof, and (iii) the compound; (b) determining the amount of the peptide bound to RAGE or the fragment thereof, and (c) comparing the amount of bound peptide determined in step (b) with the amount determined when the peptide is admixed with RAGE or a fragment thereof in the absence of the compound, thereby determining whether the compound is capable of inhibiting the interaction of the peptide with RAGE or a fragment thereof, wherein a reduction in the amount of binding in the presence of the compound indicates that the compound is capable of inhibiting the interaction.
WO2009154246A1 Therapeutic agent for erectile dysfunction Provided is a therapeutic agent for erectile dysfunction containing as the effective component a heterocyclic derivative represented by general formula (1) or a pharmaceutically acceptable salt thereof. In formula (1), R1 and R2 may be the same or different, each representing an optionally substituted aryl group; R3 and R4 may be the same or different, each representing a hydrogen atom or an alkyl group; R5 represents a hydrogen atom, an alkyl group or a halogen atom; Y represents N or N→O; A represents NR6, where R6 represents a hydrogen atom, alkyl group etc.; D represents an optionally hydroxyl group substituted alkylene or alkenylene group; E represents a phenylene group or a single bond; G represents O, S etc.; Q represents a carboxyl group, alkoxycarbonyl group etc.
US20120087971 Contact drug delivery system A drug delivery system is disclosed. The drug delivery system includes a recognitive polymeric hydrogel through which a drug is delivered by contacting biological tissue. The recognitive polymeric hydrogel is formed by using a bio-template, which is a drug or is structurally similar to the drug, functionalized monomers, preferably having complexing sites, and cross-linking monomers, which are copolymerized using a suitable initiator. The complexing sites of the recognitive polymeric hydrogel that is formed preferably mimics receptor sites of a target biological tissue, biological recognition, or biological mechanism of action. The system in accordance with an embodiment of the intention is a contact lens for delivering a drug through contact with an eye.
US20080193411 Anti-viral Compounds Disclosed are compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof of having Formula (I), their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, L1, V, W, T, Z, R, Y1, and p are as defined herein.
US20110218189 PYRROLO[2,3-d]PYRIMIDIN-2-YL-AMINE DERIVATIVES AS PKC-THETA INHIBITORS The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKCθ mediated disorders.
EP1331934B1 Ppar-alpha,beta activators for treating alopecia areata and vitiligo The invention relates to medicaments comprising activators of peroxisome proliferator-activated receptors α, β, (also known as δ), for treating skin disorders caused by auto-immune diseases or the effects of radiation, e.g. sunlight, UV light, X-rays or η rays. The invention also relates to the suppression of rejection reactions, produced by a recipient organism against transplanted tissue and to the use of said medicaments for inhibiting the effects of ageing of the skin.
WO2005027896A1 Concurrent drugs Concurrent drugs highly effective in the prevention of or treatments for thromboembolism. The drugs comprise a combination of an antiplatelet agent and a direct or selective inhibitor for activated blood coagulation factor X, the inhibitor being a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula (I) (wherein R is hydrogen or lower alkyl and Z is hydrogen or hydroxy) or a pharmacologically acceptable salt thereof. The drugs are useful in the prevention of or treatments for thromboembolism.
US20080275086 3-Amino-1-[(S)-2-(3-tert-butyl-[1,2,4]oxadiazol-5-yl)-pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)-butan-1-one; dipeptidyl-peptidase inhibitor; antidiabetic, hypoglycemic agent; metabolic disorders, obesity, non-insulin dependent diabetes The invention relates to compounds of formula (I) wherein Z, R1-7, X and n have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.
EP2230232A1 Addition salts of tromethamine with azabiphenylaminobenzoic acid derivatives as DHODH inhibitors The present invention is directed to novel crystalline addition salts of (i) tromethamine with (ii) an azabiphenylaminobenzoic acid derivatives of formula (I) wherein R1 is selected from the group consisting of C1-C4 alkyl, C3-C4 cycloalkyl and -CF3, G1 is selected from nitrogen atoms and CH, C(CH3) and C(CF3) groups, and G2 represents a phenyl group optionally substituted with one or two substituents selected from chloro, fluoro, methoxy, ethoxy, isopropoxy, trifluoromethoxy, CF3, and -CONR7R8, wherein R7 is hydrogen and R8 is cyclopropyl or R7 and R8 together with the nitrogen atom to which they are attached form a group of formula wherein n is 1. and pharmaceutically acceptable solvates thereof, and their use in the treatment, prevention or suppression of diseases susceptible to ameliorate by inhibition of dihydroorotate dehydrogenase such as autoimmune, infectious and viral diseases.
CN1883543A A cough-stopping asthma-relieving oral liquid and method for preparing same The invention provides an oral liquid for cough-relieving, which comprises 5-80% by weight or volume of active constituents of liquid extract of liquorice and potassium antimony tartrate, 0.1-3% by weight or volume of glycerol and balancing water. The proportion of liquid extract of liquorice and potassium antimony tartrate is 1-3:1-2.
US20060287353 Method for preventing or treating ischemia-or hemorrhage-induced brain damage using a macrolide compound Macrolide compound, such as a tacrolimus analogue is provided for use as a neuroprotective agent, particularly, for preventing or treating acute or chronic cerebral neurodegenerative diseases.
US20080045510 Succinate salts of 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline and crystalline forms thereof The present invention relates to succinic acid salt forms of the 5-HT1A binding agent 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline, as well as crystalline forms thereof, pharmaceutical compositions thereof, and methods of use thereof.
CN102210674B Use of indole-2,3-dione in preparation of medicines for preventing sperm malformation The invention relates to the use of indole-2,3-dione in preparation of medicines for preventing indole-2,3-dione. The indole-2,3-dione is natural or artificially synthesized, is low in toxicity and has good sperm malformation preventing effect.
WO2007029642A1 Remedy for osteoporosis with the use of retinoid x receptor-related compound It is intended to provide a novel remedy for osteoporosis. Use is made of HX531 which is synthesized as an antagonist to retinoid X receptor and has an activity of inhibiting the differentiation of adipocytes. The remedy can be used in a dosage form containing HX531 as the active ingredient.
US20120076823 Vector The present invention relates to a herpes virus vector which comprises a modified genomic sequence encoding a microRNA (miRNA) against a target sequence. The herpes virus vector may be used as or in a vaccine to prevent and/or treat a disease.
EP2229952A1 Plasma anti-diabetic NUCB2 peptide (pladin and nesfatin-1n) and uses thereof The present invention provides pladin (plasma anti-diabetic nucb2 peptide) polypeptide and functional equivalent thereof that are useful for treating diabetes. The present invention provides a method of treating diabetes by administering to a subject nesfatin-1, pladin, or a functional equivalent thereof. The present invention also provides a method of treating diabetes by administering to subject plasmin inhibitors.
WO2008026075A3 Treatment of intracellular bacterial infections with a protein kinase inhibitor or an as160 polypeptide activator Products for treating intracellular bacterial infections comprising a protein kinase inhibitor and/or an activator of AS160 polypeptide-. The protein kinase inhibitor may be a H-89 derivative.
CN101360721A Novel 2-aminopyrimidinone or 2-aminopyridinone derivatives and their use This invention relates to novel compounds having the structural formula Ia or Ib below (Ia) or (Ib) and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
WO2006068954A3 PYRAZOLO[1,5-A]PYRIMIDINE ADENOSINE A2a RECEPTOR ANTAGONISTS Compounds having the structural formula (I) are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is -C(O)- or -S(O)2-; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or -CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
EP1272175B1 N,n'-diaryl guanidines as il-8 receptor antagonists This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
WO2007103694A3 Triazine 11-beta hydroxysteroid dehydrogenase type i inhibitors Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein.
CN103169717A Application of anthracene nucleus antibiotic and its pharmaceutical salt for treating ocular inflammation The invention discloses an application of anthracene nucleus antibiotic and its pharmaceutical salt for treating ocular inflammation. The invention found that the anthracene nucleus antibiotic and its pharmaceutical salt have good effect on treatment of exogenous ocular inflammation and endogenous ocular inflammation, and especially the anthracene nucleus antibiotics can be prepared to prolonged action preparations such as a nano preparation, a microballoon preparation, liposome and hydrogel, the curative effect can be directly performed on ocular surface and eye ground, the toxicity of anthracene nucleus antibiotic is reduced, administration dosage is simultaneously enlarged through ophthalmic administration by prolonged action preparations, the duration time of drug effect is long, the medicament curative effect is stronger than that of the common preparations of the anthracene nucleus antibiotic, when the ophthalmic administration is carried out, the anthracene nucleus antibiotic has good treatment effect for exogenous and endogenous ocular surface, and eye ground inflammation, and especially has good treatment effect for the ocular surface and eye ground diseases caused by external wound, so that the problems of certain eyes inflammation with long treatment and more severe eye diseases due to eyes inflammation can be solved.
CN103476771A IL17 and IFN-gamma inhibition for the treatment of autoimmune inflammation The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
CN101011389A Application of arbidol in preparing medicaments for preventing and/or treating hepatitis B The invention relates to a method for using abedor to prepare the drug that prevents and treats hepatitis B. The external test has proved that the abedor can significantly restrain the hepatitis B.
EP2468280A1 Use of prokineticin 1 receptor agonists to promote the differentiation of epicardin+ progenitor cells The present invention discloses a prokineticin receptor-1 agonist for use for promoting the differentiation of cardial epicardin+ progenitor cells into cardiomyocytes in a subject affected with a cardiac disease and/or the differentiation of renal epicardin+ progenitor cells into vasculogenic and/or glomerular cells in a subject affected with a renal disease.
CN102793717A Application of sodium carbonate in preparing medicine for treating uterine fibroids by heat coagulation The invention discloses an application of sodium carbonate in preparing a medicine for treating uterine fibroids by heat coagulation. The invention is characterized in that the mass-volume percentage concentration of the preferred sodium carbonate is 1-2%, and the temperature is 60-70 DEG C; conducting fine needle aspiration under ultrasound guidance, injecting a sodium carbonate solution which is heated up to 60-70 DEG C and has the mass-volume percentage concentration of 1-2% into the muscles, wherein according to the size of the myoma, the drug is injected at a dose of 5-40ml every time, and ultrasonic re-examination is conducted after three months of the treatment to observe the atrophy of the myoma and determine the curative effect. The results show that after one or more heat coagulation treatment, the blood flow in the myoma is reduced, the myoma is reduced, the myoma presents strong echo fibrosis, thus it is proved that histocytes in the myoma are completely necrotic, and the myoma coating is surrounded by a cyclic hardening zone. 1680 cases of solitary uterine fibroids or multiple uterine fibroids after treated by heat coagulation interventional treatment with the sodium carbonate solution achieve the results of coagulation necrosis of myoma cells and significant atrophy effect of the myoma body, thus the application of sodium carbonate in treating uterine fibroids by heat coagulation is an ideal method for interventionally treating uterine fibroids.
US8791081 MGMT inhibitor combination for the treatment of neoplastic disorders A method of treating a neoplastic disease in a subject includes administering to neoplastic cells of the subject an MGMT inhibitor and at least one of an antimitotic agent or a DNA damaging agent.
WO2008015021A1 Treatment of endocrine dysfunction using iron chelators The invention relates to the use of an iron chelator for the treatment or prevention of pathologies due to iron loading, e.g. related to a dysfunction, in particular a reduction or inhibition, of the secretory function of cells from endocrine glands, in the human or animal body.
CN103520195A Application of clitocine in preparation of sensitizer The invention provides application of clitocine in preparation of a sensitizer for reversing tumor TRAIL (TNF-related apoptosis-inducing ligand) drug resistance. The clitocine has a molecular formula of C9H13N5O6 with the molecular weight of 287. The medicament consists of the clitocine and a preparation allowed drug excipient. The clitocine provided by the invention has a strong TRAIL sensitizing effect on liver cancer cells, colon cancer cells and breast cancer cells of various people and mice, can be used for effectively increasing the sensitivity of tumor cells to TRAIL under a lower dose, and inducing the apoptosis of the tumor cells in a synergistic action mode, so that the clitocine is a broad-spectrum effective TRAIL sensitizer, and provides a guarantee for the safety and extensive use of a TRAIL anti-tumor drug.
CN103536595A Acipimox composition tablet The invention provides an acipimox composition tablet, and belongs to the field of medicine and medicine production technology. The acipimox composition capsule comprises following raw materials and auxiliary materials, by weight, 400 parts of acipimox, 100 parts of chitosan nanoparticle, 400 parts of croscarmellose sodium, 650 parts of 4% hydroxypropyl methylcellulose 50% ethanol, 400 parts of carboxy methyl starch, and 12 parts of magnesium stearate. Advantages of the acipimox composition tablet are that: main drug solubility is improved further, that is to say, a uniform viscous suspension is obtained rapidly when the acipimox composition tablet is contacted with water, so that fine particles are obtained rapidly in gastrointestinal tract by disintegration, drug distribution area is enlarged, absorption points are increased, overhigh local drug concentration in gastrointestinal tract caused by common tablets and capsules is avoided, irritation on gastrointestinal mucosa is avoided, untoward effects are reduced, and adaptability of patients is increased. The acipimox composition tablet is convenient for patients to take; absorption speed is fast; and bioavailability is high.
US20100322855 Bimodal ligands with macrocyclic and acyclic binding moieties, complexes and compositions thereof, and methods of using Substituted 1,4,7-triazacyclononane-N,N′,N″-triacetic acid and 1,4,7,10-tetraazacyclcododecane-N,N′,N″,N′″-tetraacetic acid compounds with a pendant amino or hydroxyl group, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.
CN101780102A Medicine for treating dermatosis and preparation method thereof The invention discloses a medicine for treating dermatosis and a preparation method thereof. The medicine for treating dermatosis comprises the following raw materials by weight ratio: 50 liquor, 50 vinegar, 30-40 sulfur, 1.5-2 alumen, 1-2 borneol, 1-2 potassium nitrate and 2-3 camphor. The preparation method comprises the following steps: firstly, taking the raw materials according to the formula, and respectively crushing the sulfur, the alumen, the borneol, the potassium nitrate and the camphor to be prepared for use; secondly, putting the sulfur in the vinegar to be soaked for 12-48 hours, adding the liquor, the alumen, the borneol, the potassium nitrate and the camphor to be soaked for 0.5-3 years, filtering, and respectively collecting a liquid medicine and dregs of a decoction to obtain the medicine. Compared with the prior art, the medicine for treating dermatosis has convenient use, simple and reasonable formula, very good functions of reducing fever, eliminating stasis, diminishing inflammation, detumescence and detoxification, very good curative effect for treating psoriasis, tinea of feet and hands, finea corporis, tinea capitis, acne and other dermatosis, short period of treatment, rapid effect and no recrudescence.
US8383790 Modified surface antigen Novel proteins that constitute modified forms of a Neisseria meningitidis surface antigen and encoding nucleic acids are provided. The modified surface proteins are characterized by having deletions of non-conserved amino acids, and thereby being capable of eliciting cross-protective immune responses against Neisseria meningitidis. The invention extends to the use of the modified surface antigens in diagnostics, in therapeutic and prophylactic vaccines and in the design and/or screening of medicaments. The modified surface antigens are particularly useful in vaccines which effectively immunize against a broader spectrum of N. meningitidis strains than would be expected from a corresponding wild-type surface antigen.
US20120088723 Selective ep4 receptor agonistic substance for treatment of cancer This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.
US20080045509 Substituted benzyl amine compounds Certain substituted benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
WO2008130314A1 Xanthine compounds having a positive allosteric gabab receptor modulator effect The present invention relates to novel xanthine compounds of the general formula (I) wherein R1, R2, R3 and R4 are as defined, having a positive allosteric GABA Breceptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABA Bagonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).
US20080262071 Pindolol for the Treating Premenstrual Syndrome and Premenstrual Dysphoric Disorder In accordance with the present invention, it has been discovered that pindolol provides a highly effective treatment for PMS and/or PMDD. As such, the present invention generally relates to methods and compositions for treating and/or preventing PMS, or symptoms associated therewith including premenstrual tension or premenstrual dysphoria. The methods and compositions of the invention also involves the use of pindolol, a known beta adrenergic blocker, in combination with known contraceptives.
WO2011068288A1 Agent for prevention or treatment of benign prostatic hyperplasia comprising a quinazoline derivative The present invention provides a prophylactic or therapeutic agent for benign prostatic hyperplasia (BPH) and accompanying lower urinary tract symptoms (LUTS), comprising a quinazoline derivative as an active ingredient. Further, the present invention provides a composition comprising a quinazoline derivative for use in the treatment or prevention of BPH and LUTS, and a method for preventing or treating BPH and LUTS, including administering an agent or a composition comprising a quinazoline derivative to a mammal including a human. The BPH prophylactic or therapeutic agent or composition ofthe present invention has excellent PDE5 inhibitory effects, exhibits low inhibitory activity on PDE6 and PDE11 at a dose exhibiting PDE5 inhibitory activity, thus providing less side effects, has a moderate blood half-life as compared to other PDE5 inhibitors and therefore can exert sufficient medicinal efficacy even with single administration/day without risk of drug accumulation,thus providing increased drug compliance and excellent metabolic stability.
WO2013080265A1 Stabilization of s-adenosylmethionine with acid sodium metaphosphate A novel method for the stabilization of S-adenosylmethionine is provided. The present invention provides a composition to eat or drink, said composition containing both S-adenosylmethionine and acid sodium metaphosphate. The present invention also provides a process for preparing stable S-adenosylmethionine, said process including a step of adding acid sodium metaphosphate to a composition that contains S-adenosylmethionine. The present invention further provides a method for the stabilization of S-adenosylmethionine, said method including a step of adding acid sodium metaphosphate to a composition that contains S-adenosylmethionine.
US20110104136 Natural Killer p30 (NKp30) Dysfunction and the Biological Applications Thereof The present invention relates to a method of assessing a favourable or, on the contrary, an unfavourable prognosis of a cancer in the subject, which method comprises detecting the presence of a mutated Natural Cytotoxicity-triggering Receptor 3 (NCR3) nucleic acid, an abnormal relative amount of at least one particular Natural Killer p30 (NKp30) RNA transcript isoform, and/or an abnormal Natural Killer p30 (NKp30) expression or activity of at least one particular NKp30 protein isoform in a sample from the subject, the presence of said mutated NCR3 nucleic acid, abnormal relative amount of at least one particular NKp30 RNA transcript isoform, or abnormal expression or activity of at least one particular NKp30 protein isoform being indicative of the prognosis of said cancer in the subject.
WO2013187727A1 Phenylalkyl sulfamate compound and muscle relaxant composition comprising the same The present invention relates to novel phenylalkyl sulfamate compounds, a method for preventing or treating a disease associated with muscle spasm. The present invention ensures the enhancement of muscle relaxation activity essential for alleviation of muscle spasm, such that it is promising for preventing or treating various diseases associated with muscle spasm.
CN101225092B Manganese complex as well as preparation method and uses thereof The invention discloses a manganese complex and the preparation method and application of the manganese complex, providing a complex of manganous, 1, 10-phenanthroline and sulfate. The preparation method is to stir the manganous, 1, 10-phenanthroline and sulfate in the solvent and the complex is acquired after reaction. The preparation method for the manganese complex has the advantages of easy access to the composite material, low cost, precipitation of crystal form with high purity and high yield, stable existence in natural state, good water soluble and fat-soluble performance, excellent inhibition effect to cells of lung cancer, liver cancer, colon adenocarcinoma and a plurality of cancers, wide action spectra and application range.
WO2008072534A1 Solid medicinal preparation containing mannitol or lactose A solid medicinal preparation containing the compound of the following general formula (I) or a pharmacologically acceptable salt thereof. It has improved content evenness. The solid medicinal preparation contains: (A) the compound of the following general formula (I): or a pharmacologically acceptable salt thereof; and (B) mannitol or lactose which, when examined under specific conditions, has a particle size distribution having a particle diameter at 90% cumulation of 80-300 µm.
WO2011119610A3 (20S)-2-METHYLENE-19-NOR-22-DIMETHYL-1α,25- DIHYDROXYVITAMIN D3 AND (20R)-2-METHYLENE-19-NOR-22- DIMETHYL-1α,25-HYDROXYVITAMIN D3 Compounds of formula I are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
US20120093923 Apparatus And Methods For Delivering A Plurality Of Medicaments For Management Of Co-Morbid Diseases, Illnesses, Or Conditions A method and apparatus for delivering a plurality of medicaments in a single delivery vehicle for the management of co-morbid diseases, illnesses and conditions. The present invention provides a novel delivery process for many medicaments. Medicaments may be encapsulated and stored separately within a larger capsule until the time of ingestion, consumption, or the like. Benefits of the present invention include maintaining separation of distinct ingredients within a single capsule and the capability to control the time release of multiple ingredients within the capsule.
CN102247505A Chinese medical composition for treating sterility of multiparous cow after repeated mating and treatment method of sterility of multiparous cow after repeated mating The invention relates to a Chinese medical composition for treating the sterility of a multiparous cow after repeated mating, comprising the following components in parts by weight: 25-35 parts of deerhorn gelatins, 55-65 parts of radix morindae officinalis, 25-35 parts of angelica sinensis, 25-35 parts of rhizoma ligustici wallichii, 25-35 parts of radix rehmanniae preparata, 10-20 parts of bighead atractylodes rhizome, 25-35 parts of prepared rhizoma cyperi with vinegar, 15-25 parts of saute fennel, 55-65 parts of fructus psoraleae, 25-35 parts of dogwood fruits, 55-65 parts of dangshen, 15-25 parts of actinolite, 1-10 parts of radix aconiti carmichaeli and 10-20 parts of liquorices. The Chinese medical composition provided by the invention has the effects of nourishing yin and supplementing blood, harmonizing ying blood, assisting kidney yang, warming meridians to dissipate cold, warming womb, warming the kidney yang and supplementing life-gate fire, can be used for treating the sterility of the cow, caused by blood deficiency and womb cold, and can also promote the oestrus of the cow and increase the conception rate by matching with hormone drugs such as stilboestrol and the like.
CA2263846C Novel pyranoside derivatives The present invention relates to new pyranoside derivatives of general formula I, processes for preparing them and their use in pharmaceutical compositions.
US20080317873 Pain Relief Compositions A pain relieving composition for topical application is provided that includes magnesium sulfate (Epsom salts). The composition provides magnesium sulfate in an amount effective for providing pain relief. The composition has a viscosity effective for allowing topical application of the composition to an afflicted area where the magnesium sulfate is absorbed through the skin to provide pain relief. The composition provides the novel benefits of being portable, easily dispensed, and provides a higher concentration of applied magnesium sulfate than the traditional dispensing method of soaking solutions.
US20080026054 Novel anelgesic combination The invention discloses a method of administering a pharmaceutical combination comprising an NSAID and a slow release tramadol to a mammal in need of thereof. This invention further discloses an analgesic combination comprising an NSIAD and a slow release tramadol for treating pain and pain related conditions.
WO2013007003A1 Novel use of acetylacetic acid for regulating proliferation of skeletal-muscle cells Disclosed is the use of acetylacetic acid in preparing drugs for promoting the proliferation of skeletal-muscle cells, the skeletal-muscle cells being myoblasts, wherein the acetylacetic acid promotes the proliferation of the skeletal-muscle cells by activating the ERK pathway so as to up-regulate the expression of a cyclin, such as cyclin D1. Also disclosed is the use of acetylacetic acid in preparing drugs for treating injuries to skeletal muscle, and a drug composition for promoting the proliferation of skeletal-muscle cells, containing acetylacetic acid and Insulin-like Growth Factor 1.
WO2011055142A2 1,4-quinones and their sulfur analogues useful as ligands of n-acetyltransferases The invention provides 1,4-quinones, 1,4-naphthoquinones and their sulphur analogues as inhibitors of hNAT1, an enzyme which is both a diagnostic marker and drug target for breast cancer. Some of the compounds of the invention are also chromogenic in the presence of hNAT1. The compounds of the invention are used for detecting for and/or measuring hNAT1 and for inhibiting hNAT1 in the treatment of disease.
US7507831 Therapy for breast cancer; plant extracts; 4-[(2-benzothiazolyl)thio]-5,7,3',4'-tetra-O-benzyl-epicatechin, 4-[(2-benzothiazolyl)thio]-5,7,3',4'-tetra-O-benzyl-catechin, 4-[(2-benzothiazolyl)thio]-3-O-acetyl-5,7,3',4'-tetra-O-benzyl-epicatechin Various processes are disclosed for preparing protected epicatechin oligomers having (4β,8)-interflavan linkages. In one process, a tetra-O-protected epicatechin monomer or oligomer is coupled with a protected, C-4 activated epicatechin monomer in the presence of an acidic clay such as a mortmorillonite clay. In another process, a 5,7,3′,4′-benzyl protected or a 3 -acetyl-, 5,7,3′,4′-benzyl protected epicatechin or catechin monomer or oligomer is reacted with 3 -O-acetyl-4-[(2-benzothiazolyl)thio]-5,7,3′,4′-tetra-O-benzylepicatechin in the presence of silver tetrafluoroborate. In another process, two 5,7,3′,4′-benzyl protected epicatechin monomers activated with 2-(benzothiazolyl)thio groups at the C-4 positions are cross-coupled in the presence of silver tetrofluoroborate. A process is also disclosed for reacting an unprotected epicatechin or catechin monomer with 4-(benzylthio) epicatechin or catechin. The use of naturally-derived and synthetically-prepared procyanidin (4β,8)4-pentamers to treat cancer is also disclosed.
US7183261 Galactosylceramide analogs, and β-glucocerebrosidase activators, external skin preparations and method of activating β-glucocerebrosidase using the analogs Galactosylceramide analogues represented by the following formula (1) or (2). (wherein X and Y each represent S or O, R1 and R2 each represent an alkyl group or an alkenyl group each having 9 to 35 carbon atoms. R3 represents an alkyl group or an alkenyl group each having 2 to 30 carbon atoms.) It is provided a β-glucocerebrosidase activator which is easily available, and external skin preparations and a method of activating β-glucocerebrosidase, in which improvement in formation of horny layer transmission barrier is expected by activating β-glucocerebrosidase so that an improved effect in rough skin is also expected.
EP0596049B1 Defoaming composition A defoaming or antifoaming composition comprises a free flowing granular combinate of 50 to 90 weight percent of a water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin agglomerates, maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbito agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids and about 10 to 50 weight percent of a liquid, non aqueous, defoaming or antifoaming composition such as simethicone, hydrocarbon-based oils or silicone oils. The composition may be combined with one or more suitable excipients and prepared as a unit dosage in the form of a compressed tablet, filled capsule, packet, or granule for various defoaming applications.
WO2007053498A1 Compounds useful as antagonists of ccr2 The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.
WO2013139387A1 Stabilized pharmaceutical compositions comprising rasagiline salts The invention deals with processes of making stable and content uniform solid pharmaceutical compositions comprising a salt of rasagiline with L-tartraric or fumaric acid as the active ingredient. As a result of such process, a stable and content uniform pharmaceutical composition comprising rasagiline L-tartrate or fumarate and L-tartaric acid is provided.
EP1373206B1 Aryl oxime-piperazines useful as ccr5 antagonists In one embodiment, this invention provides a novel class of aryl oxime-piperazine compounds as antagonists of the CCR5 receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more of diseases associated with the CCR5 receptor. An illustrative inventive compound is shown below: (Formula I).
US20100120707 Dosages for menstrual suppression, contraception, and hormone replacement therapy, and methods of administering same A dosage comprising an antibiotic, an estrogen, and a progestagen is provided. The dosage can be oral, or administered in other methods, such as intravaginally with a tampon. The dosage can be used for menstrual suppression, contraception, and/or hormone replacement therapy. A method of treating a patient with the dosage comprises administering the dosage to the patient over a course of treatment, in amounts or frequencies that can remain constant, or be varied.
WO2013050884A1 Process for the preparation of lersivirine The present invention relates to a process for the preparation of lersivirine or a pharmaceutically acceptable salt thereof characterised in that it uses the base 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) and the solvent acetonitrile.
US20080138440 Methods of diagnosing and alleviating gadolinium toxicity The present invention relates to novel methods of treating or reducing the likelihood of developing gadolinium toxicity by administering to a patient a metal chelator before, concurrently with, or after exposure to gadolinium. The novel methods comprise, inter alia, the use of iron chelators to aid patients at increased risk of developing a gadolinium-induced condition, such as nephrogenic systemic fibrosis, acute kidney injury, cardiovascular disease and accelerated senescence.
CN102225142A Itch relieving ointment for women The invention relates to an itch relieving ointment for women. The ointment is prepared by decocting the following raw materials: 10 to 40 parts of motherwort, 20 to 30 parts by weight of white peony root, 10 to 20 parts by weight of radix bupleuri, 10 to 30 parts by weight of Poria cocos, 20 to 40 parts by weight of gentian, 10 to 20 parts by weight of Chinese angelica, 10 to 20 parts by weight of cordate houttuynia, 5 to 10 parts by weight of bighead atractylodes rhizome, 5 to 15 parts by weight of sophora flavescens, 5 to 10 parts by weight of Cyperus rotundus, 5 to 15 parts by weight of Ligusticum wallichii, 5 to 10 parts by weight of cape jasmine and 1 to 2 parts by weight of borneol. According to the invention, the raw materials are carefully chosen and reasonably combined; the ointment has no toxic and side effects, is easy and convenient to use, and produces good treatment effects and a quick curative effect.
US20110256117 Manufacturing and use of composite scaffolds The present invention refers to a method of manufacturing a composite scaffold including the surface grafting of the scaffold using gamma-irradiation as well as gamma-irradiation of a polymer contacted with the surface of the scaffold. The present invention also directed to the use of the scaffold for tissue engineering and other applications. The present invention is further directed to a method of culturing cells in a composite scaffold of the present invention and to a three-dimensional porous composite scaffold.
CA2315261C Oral pharmaceutical extended release dosage form An enteric coated pharmaceutical extended release dosage form of an H+,K+-ATPase inhibitor giving an extended plasma concentration profile of an H+,K+-ATPase inhibitor. The extended plasma profile is obtained by a pharmaceutical composition which comprises a core material of a hydrophilic or hydrophobic matrix, and the H+,K+-ATPase inhibitor and optionally pharmaceutically acceptable excipients. The dosage form may be administered once daily.
CN102028698A Medicine for treating colon cancer and preparation method thereof The invention discloses a medicine for treating colon cancer and a preparation method thereof, comprising effective medicine ingredients: 3beta-hydroxy-28-nor-ursol-17, 19, 21-triene and medicament prepared from pharmaceutic adjuvants. The medicine comprises the following components by weight percent: 1% to 90% of effective ingredients and 10% to 99% of the pharmaceutic adjuvants.. The structural formula of the effective ingredient of the medicine is C29H44O. The preparation method of the medicine for treating colon cancer comprises the following steps: (1) adding charred radix sanguisorbae taken as a raw medicine material into carbinol or ethanol for repeated extraction, and obtaining fluid extract by filtration; (2) dispersing the fluid extract of the first step with water, and carrying out chloroform extraction, and recycling solvent of the extract liquid to obtain extract; (3) crystallizing solid which is obtained by carrying out the suction filtration on extract of the second step to obtain the effective ingredients of compound medicine; (4) taking the effective ingredients of the medicine according to the weight ratio, and wherein the rest pharmaceutic adjuvants are prepared into the medicament. The medicine disclosed by the invention is mainly used for treating colon cancer without metastasis symptom and allaying pain of patients in the chemotherapy period after the operation, and has non-toxic side effects.
CA2719907A1 Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists The present invention provides compounds of Formula I, pharmaceutical compositions thereof, and method of us-ing the same in the treatment or prevention of diseases mediated by the activation of .beta.3-adrenoceptor.
US20090258049 Drug eluting expandable devices The present disclosure relates to drug eluting devices, and their uses. The drug eluting devices can allow for perfusion during deployment. The coatings the may contain bioactive materials which elute once deployed in a patient and can have anti-proliferative, anti-inflammation, or anti-thrombotic effects. Sol gel technology can be used to coat the devices.
US20080234284 Pyrazolo[1,5-a]Pyrimidin-7-Yl Amine Derivatives as Protein Kinase Inhibitors The invention relates to pyrazolo[1,5a]pyrimidin-7-yl amine derivatives of formula (I) and salts thereof, their use in the treatment of protein kinase dependent diseases.
CN103381165A Applications of Chukrasone A in anti-helicobacter pylori medicines In vitro activity experiment indicates that Chukrasone A has excellent inhibitory activity on helicobacter pylori (Hp). Chukrasone A can be used for treating diseases such as acute and chronic gastritis, gastric ulcer and duodenal ulcer, and in preparation of medicines used for treating acute and chronic gastritis, gastric ulcer and duodenal ulcer. Applications of Chukrasone A in preparation of medicines used for treating helicobacter pylori are disclosed for the first time. Due to the fact that skeleton type belongs to completely novel skeleton type, and inhibitory activity of Chukrasone A on helicobacter pylori is unexpectedly high, probability of other compounds giving any revelation for Chukrasone A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in treating and preventing helicobacter pylori.
US20070253943 Compositions for Topical Treatment Compositions are disclosed for topical treatment of mammalian skin, particularly human skin, relieve the distressing symptoms of the many skin diseases and provide, in many cases, a long term cure. The composition comprise, in combination, one or more boswellic acids and/or a fatty acid having a chain length of at least 18 carbon atoms and which contains at least two unsaturated linkages together with an enzyme based antibacterial system. The compositions will selectively reduce cell turnover and may be used for the treatment of eczema and/or psoriasis.
US20100316693 Method for preparing an antimicrobial cotton of cellulose matrix having chemically and/or physically bonded silver and antimicrobial cotton prepared therefrom There is provided a method for preparing a natural cellulose-AgO matrix having antimicrobial activity without leaching silver from the cellulose-AgO matrix. The method comprises: introducing silver ions (Ag+) into a natural cellulose matrix by dipping the natural cellulose matrix in an AgCl-dissolved NH4OH solution; and substituting hydrogen (H) of hydroxyl group (—OH) in natural cellulose with Ag+ by drying the silver ion-infused natural cellulose matrix, thus to form a natural cotton-AgO complex. The cellulose-AgO matrix prepared in the method may be useful to continuously maintain antimicrobial activity by maintaining an effective concentration of silver, which does not have cytotoxicity to human skin, and chemically bonded silver is not leached during the rehydration due to the chemical bond between the silver and the cellulose matrix.
US7132452 Useful for threapy of pain/inflammation associated with infection caused by herpes virus, especially herpes simplex virus (HSV) and varicella-zoster virus (VZV) The present invention provides a topical formulation containing NSAID, particularly diclofenac. The topical formulation is particularly useful for alleviating pain/inflammation associated with infection caused by herpes virus, especially herpes simplex virus (HSV) and varicella-zoster virus (VZV). Similar relief can be achieved where diclofenac is replaced with another non-steroidal anti-inflammatory drug (NSAID), which includes, without limitation, etodolac, ketorolac, bromfenac, diflunisal, ibuprofen, fenoprofen, ketoprofen, naproxen, suprofen, meclofenamate, mefenamic acid, piroxicam, meloxicam, indomethacin, sulindac, phenylbutazone, oxyphenbutazone, and tolmetin. The topical formulation is further characterized by its fast relief on pain and/or inflammation associated with infection caused by herpes virus, i.e., a complete relief in no more than seven (7) days after the application of the topical formulation on skins of patients.
US20080176925 Toluene sulfonic acid salt of a therapeutic compound and pharmaceutical compositions thereof The present invention is directed to the tosylate salt of trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide (1): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.
US20080063706 Methods and Medicaments for Administration of Ibuprofen A method for administration of ibuprofen to a subject in need of ibuprofen treatment is provided, in which an oral dosage form comprising a therapeutically effective amount of ibuprofen and a therapeutically effective amount of famotidine is administered three times per day.
CN101318930A Herbimycin derivant, preparation method and antineoplastic application thereof The invention relates to a herbimycin derivative shown in formula (1) with R1 being OCH3 and R2=R3 being OH, and relates to a preparation method of the derivative and an application in anti-tumor of the derivative acting on heat shock protein. The invention is characterized in that a compound (herbimycin A) with R1=R2=R3 being OCH3 shown in the formula (1) is subject to microbial transformation through Eupenicillium javanicum; the solubility of a herbimycin derivative which is obtained through a structural modification in water is one order of magnitude more than that of the herbimycin A, and the herbimycin derivative has strong in-vitro anti-Hela tumor cells activity and in-vitro anti-Ehrlich tumor cells activity, wherein, IC 50 of the Hela tumor cells and IC 50 of the Ehrlich tumor cells are 5.8 mug.mL<-1> and 0.7 mug.mL<-1> respectively.
CN101530400A Effervescence tablet capable of treating penis erection dysfunction and preparation method thereof The invention provides an effervescence tablet capable of treating penis erection dysfunction and preparation method thereof. The raw medicine of the effervescence tablet is 5 type phosphodiesterase (PDE5) selective inhibitor special for cyclic guanosine monophosphate (cGMP) wherein the active ingredient is invariant. The effervescence table is formed using effervescence material as disintegrating agent and generates a large amount of air bubbles in water. The effervescence tablet dissolves in shorter time with features of quick medicine effect, high bioavailability, convenient carryover, especially suitable for quick administration and patient incapable of swallowing solid preparation. The preparation method is simple and convenient.
CN103550267A Folium ginkgo soft capsule and preparation method thereof The invention relates to a folium ginkgo soft capsule and a preparation method thereof, and belongs to the technical field of a pharmaceutical preparation. The folium ginkgo soft capsule consists of a content and a soft capsule shell, wherein each mg of folium ginkgo extract contains 0.36-0.46mg of total flavonoid glycoside, and terpene lactone in each mg of the folium ginkgo extract accounts for 0.09-0.13mg in terms of total content of bilobalide, ginkgolide A, ginkgolide B and ginkgolide C. The folium ginkgo soft capsule disclosed by the invention, different from a normal soft capsule, has obvious characteristics of stable nature, long storage time, short disintegration time, quick dissolving and the like.
US20070270381 Using phosphonium compound; therapy for oxidative stresses The invention provides mitochondrially targeted antioxidant compounds. A compound of the invention comprises a lipophilic cation covalently coupled to an antioxidant moiety. In preferred embodiments, the lipophilic cation is the triphenyl phosphonium cation, and the compound is of the formula P(Ph3)+XR.Z- where X is a linking group, Z is an anion and R is an antioxidant moiety. Also provided are pharmaceutical compositions containing the mitochondrially targeted antioxidant compounds, and methods of therapy or prophylaxis of patients who would benefit from reduced oxidative stress, which comprise the step of administering the compounds of the invention.
WO2008120264A1 Use of misoprostol for the topic treatment of skin lesions by stings and burns A pharmacological preparation of misoprostol for the treatment of skin lesions from insect bytes and stings and superficial burns in the form of ointment, cream, gel and paste, wherein the misoprostol is present in an amount comprised between 10 and 25 mg per gram of preparation.
CA2797752A1 Methods of designing, preparing, and using novel protonophores The present invention provides a computer-assisted method of generating a protonophore requiring the use of a computer including a processor. The method includes: designing the protonophore, calculating, using the processor, an estimatedprotonophoric activity; producing the protonophore if the estimated protonophoric activity corresponds to an U50 of about 20 µM or less; and determining the uncoupling activity of the protonophore. The present invention also provides novel protonophores that meet the above requirement and their methods of use. The present invention further provides pharmaceutical compostions/pesticides/ fungicides containing protonophore.
CN1903219A Abalone shell calcium complement agent and its prepn. method A Ca supplement for increasing bone density and protecting eye and liver is prepared from the shell of abalone through washing with the solution of sodium hypochlorite and pulverizing to obtain powder.
CN102872129A Application of Houttuynoid E in drug for treating endometrial cancer The invention discloses application of Houttuynoid E in preparing a drug for treating endometrial cancer, belonging to the technical field of the new use of the drug. Houttuynoid E is found to have obvious inhibition effect on the growth of human endometrial cancer cell lines ISK and RL95-2 through MTT (Methyl Thiazolyl Ternzolinm) anticancer activity evaluation in vitro. Therefore, Houttuynoid Ecan be used for preparing the anti-endometrial cancer drug and has excellent prospects in development and application. The use of Houttuynoid E in preparing the drug for treating the endometrial cancer involved in the invention is disclosed for the first time; the framework type of Houttuynoid E is a brand new framework type; and Houttuynoid E has an unexpectedly high inhibition activity for the endometrial cancer cells.
WO2007148832A1 Skin whitening agent containing zinc as active ingredient Disclosed is a skin whitening agent having a good feeling of use. Specifically disclosed is a skin whitening agent composed of a zinc pyrrolidone carboxylate salt. Also disclosed are a cosmetic composition for skin and an external preparation for skin, which are characterized by containing the skin whitening agent.
CN101199475A Lincomycin hydrochloride sustained-release preparation and process for preparing same The invention relates to drug preparation field, in particular to a sustained-release preparation of a lincomycin hydrochloride, which is characterized in that the invention is composed of the following ingredients based on weight percentage: forty-eight to sixty-eight percent of lincomycin hydrochloride, thirty to fifty percent of sustained-release materials, and the rest is other medicinal auxiliary material. The invention also discloses the related preparation method for the sustained-release preparation.
US7622471 Pyrazole derivatives having a pyridazine and pyridine functionality The present invention is directed to a strong platelet aggregation-inhibiting agent which does not inhibit COX-1 or COX-2. Further, the present invention provides compounds represented by formula (I), salts of the compounds, and solvates or hydrates of the compounds or the salts. Also provided are medicaments containing any of the compounds, salts, or solvates and preventive and/or therapeutic agents for ischemic diseases, containing any of the compounds, salts, or the solvates or hydrates.
US6899896 Hydrogel-driven layered drug dosage form A controlled release dosage form for sertraline has a core comprising a sertraline-containing composition and a water-swellable composition wherein the water-swellable composition is in a separate region within the core. A coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. In one embodiment, the dosage form releases sertraline to the use environment at an average rate of 6 to 10 wt % per hour from the second to the twenth hour after introduction to a use environment and less than about 25 wt % for the first two hours and at least 70 wt % by the twelfth hour, where the percentages correspond to the mass of drug released from the tablet divided by the total mass of drug originally present in the tablet. In another embodiment, the dosage form releases less than about 25 wt % of sertraline to the use environment by the second hour after introduction of the dosage form to the use environment, and delivers at least 25 wt % from the eighth to the twenty-fourth hour.
EP1237904B1 14,15-beta-methylene substituted androgens The disclosed invention relates to the unexpected finding of novel steroids which are characterized by a 14 beta ,15 beta -cyclopropane ring and a 17 alpha hydroxymethyl group. These steroids according to the invention are found to have in common an androgenic activity. They can be used for the preparation of an agent for male contraception, as well as for the preparation of a medicament for the treatment of androgen insufficiency.
WO2010118339A3 Formulations of indole-3-carbinol derived antitumor agents with increased oral bioavailability A pharmaceutical composition for treating, inhibiting, or preventing cancer can include an indole-3-carbinol derivative compound in a pharmaceutically acceptable carrier that is configured for oral administration. The indole-3-carbinol derivative compound can have antitumor activity, and oral administration can provide blood bioavailability of about 0.5% to about 25%. The pharmaceutically acceptable carrier can include a hydroxyl-fatty acid PEG monoester and/or diester. The carrier can be a hydroxyl-fatty acid PEG ester that includes 12-hydroxy stearate. The carrier can be a hydroxyl-fatty acid PEG ester that includes a PEG having from about 100 MW to about 200,000 MW. The indole-3- carbinol derivative can be 2,10-dicarbethoxy-6-methoxy-5,7-dihydro-indolo-(2,3- b)carbazole.
CN1631360A Freeze dried injection of lysine hydrochloride and its preparation process Disclosed is a Lysine hydrochloride freeze dried preparation, which comprises Lysine hydrochloride 1-5g and at least one pharmaceutically acceptable carrier, which includes excipient, pH modifier, anti-oxidant agent, stabilizer, and is provided in the form of unit amount in the container. The advantages of the invention include easy medicament transport and preservation, and prevention of freezing of the liquid injection in winter.
EP2331504A2 Piperidylpropionamide derivatives useful for the treatment of cns disorders including depression and panic disorder This invention relates to novel piperidine-4-propionamide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
CN1568985A Orally disintegrating tablet of Huperzine A and its preparation The invention discloses an orally disintegrating tablet of Huperzine A and its preparation, by using water-soluble and/or water-insoluble findings as bulking agent, adding crumbling agent, binding agent, lubricating agent, flavoring agent, aromatic, and flow aid, the tablet is prepared through granulation and pelleting.
CN103751734A Blood circulation invigorating and pain relieving adhesive plaster and preparation method thereof The invention discloses a blood circulation invigorating and pain relieving adhesive plaster. The blood circulation invigorating and pain relieving adhesive plaster comprises 1-20 parts by weight of medicinal active components and 60-100 parts by weight of a matrix, and the matrix is prepared by using the following raw materials, by weight, 10-80 parts of carbomer, 10-100 parts of polyvinylpyrrolidone K30, 20-120 parts of gelatin, 10-80 parts of sodium polyacrylate, 0.1-5 parts of disodium ethylene diamine tetraacetate, 80-200 parts of glycerin, 1-5 parts of ethylparaben, 1-10 parts of ethanol and 150-300 parts of water. The blood circulation invigorating and pain relieving adhesive plaster has the advantages of substantial drug effects, easy absorption, small irritation to skins, repeatable uncovering and application, safe production and good stability.
US20100047344 Performance enhancing composition and use thereof The performance of a mammal, manifested as a reduced oxygen uptake (VO2) during physical exercise, can be enhanced by administering to said mammal a non-toxic amount of nitrate and/or nitrite. Liquid, semi-solid and solid snack and food products and nutritional supplements, such as sport drinks are made available.
WO2012174095A1 3-desoxy-2-methylene-19-nor-vitamin d analogs and their uses This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-l a,25-diydroxy-19-nor-vitamin D3 and (20R)-3- desoxy-2-methylene-la,25-dihydroxy- 19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.
CN1762352A Phentolamine mesylate pills and its preparation method The invention relates to a Phenpolamine drop pill and its preparing process, wherein the drop pill comprises Phenpolamine as the reactive composition as well as matrix. The preparing process consists of raw material disintegrating, grinding, heating the matrix, charging Phenpolamine, stirring homogeneously, instilling into condensate liquid for cooling down and forming.
CA2503945A1 Composition for regulating bone metabolism The present invention provides a composition for regulating bone metabolism that comprises proanthocyanidins. It is preferable that the proanthocyanidins in this composition for regulating bone metabolism are contained in an extract derived from a natural product, and the extract comprises at least 20 wt% of oligomeric proanthocyanidins having a degree of polymerization of 2 to 4 in terms of dry weight. The composition of the present invention provides an effect of regulating bone metabolism.
CN103239494A Nasal spray composition for treating migraine and preparation method thereof The invention relates to a nasal spray composition for treating migraine and a preparation method thereof. The nasal spray composition is prepared from the following raw materials in parts by weight: 100 to 150 parts of ligusticum wallichii, 10 to 50 parts of asarum sieboldii, 100 to 150 parts of radix angelicae and 0.2 to 1 part of borneol. The nasal spray composition is characterized in that the ligusticum wallichii, the asarum sieboldii and the radix angelicae are prepared into essential oil and/or aromatic water; and the borneol is prepared into a borneol solution. In addition, the nasal spray composition further comprises a solubilizer with the volume ratio of 4.5% to 6%, a corrosion remover with the volume ratio of 0.1% to 0.2% and the balance of water. At present, the nasal spray preparation special for treating the migraine is not provided in clinical; and the oral administration is adopted in the most of time. The medicine administration through the nasal cavity can directly effect on a diseased position without passing through gastrointestinal tracts. In general, the required dosage of the nasal spray composition is only about one tenth or one fifteenth of that of an oral medicine; and the first-pass effect of the oral medicine is avoided. The nasal spray composition is high in bioavailability and convenient in medicine administration. According to the preparation method, by selecting the effective active medicine ingredients and improving the medicine concentration, the nasal spray which is convenient to use and carry is prepared.
CN101554399A Psoralea corylifolial extract with immunologic enhancement and application thereof The invention provides a psoralea corylifolial total glycoside extract which mainly contains 40 to 50 percent of psoralea corylifolial glycoside as well as 40 to 50 percent of isopsoralen glycoside. The psoralea corylifolial total glycoside extract and dressing or excipient allowed in pharmaceutics are prepared into any preparation formulation disclosed in pharmaceutics and can also be matched with other medicines or components to be prepared into a preparation together for use. Proved by pharmacological test, the psoralea corylifolial total glycoside and the psoralea corylifolial glycoside and the isopsoralen glycoside contained thereof can all resist the reduction of leucocyte caused by cyclophosphamide and have remarkable immunologic enhancement, and can be applied to the preparation of the medicines for increasing leucocyte.
CN102336788A Glucosamine double salt for proton pump inhibitor The invention discloses a novel double salt for a proton pump inhibitor, i.e., a glucosamine double salt for a proton pump inhibitor. The proton pump inhibitor is selected from omeprazole, S-omeprazole, lansoprazole, rabeprazole and leminoprazole. The invention is characterized in that: hip joint injury of a patient caused by long-term use of the proton pump inhibitor can be avoided; and the double salt can be prepared into an injection, an enteric preparation and a quick release preparation, and can be prepared into a compound preparation together with sodium bicarbonate magnesium oxide or magnesium hydroxide and the like.
CN103751189A Pharmaceutical composition for treating rhinitis The invention provides a pharmaceutical composition for treating rhinitis. The pharmaceutical composition contains sodium cromoglycate, naphazoline hydrochloride and chlorpheniramine maleate. The composite is a spraying agent, active ingredients in the preparation can realize fast onset of action by rapid absorption through nasal mucosa, and the composition has the advantages of high bioavailability, good compliance, convenience in carrying and use and the like.
US20100227866 Tetrahydroisoquinolin-1-one derivative or salt thereof [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). [Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
WO2010036773A8 Deuterated 1-aryl-2 -aminomethyl cyclopropane carboxyamide derivatives This invention relates to novel compounds that are 1 -aryl-2-aminomethyl cyclopropane carboxyamide derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 1 -aryl-2-aminomethyl cyclopropane carboxyamide derivatives that are derivatives of milnacipran. This invention also provides pyrogen free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a norepinephrine/serotonin reuptake inhibitor (NSRI), such us milnacipran.
EP2260849A1 Compositions and methods of use for tyrosine kinase inhibitors to treat pathogenic infection Compositions and methods are provided for using tyrosine kinase inhibitors to treat pathogenic infection. In particular, methods for using Abl-family tyrosine kinase inhibitors to treat pathogenic infection are provided. Infections to be treated according to the present invention include, particularly, those caused by microbial pathogens such as bacteria and viruses.
WO2014003694A1 Synthesis of thiosemicarbazides and triazoles derived from etodolac A novel series of new etodolac hydrazide derivatives, 1 -[2-(1,8-diethyI- 1,3,4,9- tetrahydropyrano[3,4-b]indol-1 -yl)acetyl]-4-alkyl/aryl thiosernicarbazides [SGK224-230, SGK313] and 5-[(l,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl)methyl]-4- subsrituted-2,4-dihydro-3H-1,2,4-triazole-3-thiones [SGK238-244, SGK315] have been synthesized in this study.
CN1989136A 3-[4-(6-{4, 5-dihydroisoxazol -3-yl} pyridin-3-yl)- 3-phenyl]-5 -(1h-1, 2, 3-triazol -1-ylmethyl)-1, 3-oxazolidin- 2-ones as antibacterial agents Compounds of the formula (I) or a pharmaceutically- acceptable salt or pro-drug thereof: wherein R<1> is selected for example from hydrogen, halogen, optionally substituted methyl; R<2> and R<3> are independently selected from hydrogen, fluoro, chloro and trifluoromethyl;R<4> and R<5> are independently selected, for example, from hydrogen, methyl, optionally substituted (2-4C)alkyl , C(O)R<6 >or R<4> and R<5> together with the nitrogen to which they are attached form an optionally substituted 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring or an optionally substituted imidazole ring. Methods for making the compounds of formula (I), compositions containing them and their use as antibacterial agents are also described.
WO2007010012A3 Combination of a pyrimidylaminobenzamide and an mtor kinase inhibitor The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) an mTOR kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.
US8188259 Seven or more contiguous ribose groups linked by achiral 5' to 3' internucleoside phosphate linkages; antisense agents for gene expression inhibition of a wide variety of pathological disorders such as autoimmune diseases; suitable for oral administration The present invention relates to methods and compositions containing oligonucleotides suitable for administration to humans and other mammals.
CN1579381A Decanoy-acetaldehyde sodium for injection and its preparation process The invention is an injective houttuynine sodium bisulfite and its manufacturing process. The new houttuynine sodium bisulfite is made up of new houttuynine bisulfite and sodium bisulphate, because the new houttuynine sodium bisulfite is oil and insoluble in water, thus the method increases its solubility after being add-on, it is easy to be separated out in solution dynamic reservation process, causes ill reaction, it is sensitive to light, and it can cause the medicine bad. It includes: houttuynine sodium bisulfite, which is added with excepient and produced into asepsis freeze-dry product, its weight shares are: houttuynine sodium bisulfite 1-100, excepient 20-90, pH value is 2.0-9.0, the character is white or similar to white, soluble, after it is dissolved, acquires the colorless or yellow transparent liquid, it represents red when reacting with ferric chloride.
CN1965845A Drop pills of ginsenoside monomer and preparation process thereof The invention relates to a gen-seng saponin monomer drop, wherein it comprises 30-40% carbowax 4000, 45-56% carbowax 6000, and 14-15% gen-seng saponin monomer. And the production comprises that: a, heating and fusing carbowax 6000 completely, stopping heating and holding temperature at 75-85Deg. C; b, adding gen-seng saponin monomer, mixing uniformly, dissolving it into carbowax 6000; c, adding carbowax 4000, heating and holding temperature at 75-85Deg. C; d, mixing gen-seng saponin monomer and carbowax uniformly for 15-25min; e, dropping said gen-seng saponin monomer. The invention has complete adsorption and better effect, with simple operation and low cost.
US7754735 such as 3-(2-chloro-4-quinolinyl)-2,5-dimethyl-1H-indole-1-acetic acid, used for treating respiratory system disorders and as inhibitors of G protein-coupled receptor chemoattractant homologous receptor expressed on lymphocyte cells (CRTH2) The present invention relates to substituted indoles of formula (I), useful as pharmaceutical compounds for treating respiratory disorders.
WO2005020989A1 Cancer treatment with epothilones The present invention relates to an in vivo regimen for the treatment of a proliferative disease, preferably a tumor that is refractory to treatment with one or more chemotherapeutics other than a epothilone, where an epothilone is administered in a loading dose followed by at least 1 maintenance dose.
EP1853612A1 Purification of rapamycin Purified rapamycin and a chemical process for obtaining the purified rapamycin are described.
WO2011061590A1 Novel carboxamide derivatives as hiv inhibitors The present invention relates to carboxamide derivatives of Formula (I), where B1, B2, X, L, n, R, R1, R2, Z1, Z2, Rx and Ry are as defined in the claims, as compounds and compositions for inhibiting Human Immunodeficiency Virus (HIV) and process for making the compounds.
CN1634131A Disinfecting and sterilizing fomulation for vaginal mucosa The invention discloses a disinfecting and sterilizing fomulation for vaginal mucosa, which comprises Cydiodini, diluent, crumbling agent, acid forming agent, and binding agent. The invention can be applied for effectively eradicate various microorganisms with stable physical and chemical property but no irritating action.
US20080194536 Cyanoarylamines The present invention relates to a compound represented by the following formula: (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or a combination thereof, wherein Ro, R1, R1′, R2, R2′, R3 and n are defined herein. The present invention further relates to a method of treating a patient from endometreosis or uterine fibroids.
CN102895493A Blended medicine for respiratory diseases of chicken and preparation method thereof The invention provides a blended medicine for respiratory diseases of chicken. Taken by a hundred of chicken, the blended medicine comprises the following ingredients by weight: 30-50g of radix bupleuri, 30-50g of herba schizonepetae, 30-50g of pinellia tuber, 30-50g of Indian buead, 30-50g of liquorice, 30-50g of the bulb of fritillary, 30-50g of radix platycodi, 30-50g of almonds, 30-50g of figwort root, 30-50g of red paeony root, 30-50g of mangnolia officinalis, 30-50g of tangerine peel, 6-10g of wild ginger, 100-150g of gypsum, 25-45g of pinellia tuber, 80-100g of radix platycodi, 50-70g of fructus forsythiae and 50-70g of chrysanthemum. The blended medicine has the following beneficial effects that the blended medicine is simple in proportioning, is convenient to use, has a wide raw material source, lower cost and low side effect and can be blended with feeds; the effective rate is 82.6%; and the good rate is 90.7%.
US20100204189 Methods and Compounds for Vitamin D Therapy Methods and compositions comprising 1,25-dihydroxyvitamin D2 are disclosed. A method for lowering or maintaining lowered serum parathyroid hormone in human patients including administering to said patients an effective amount of 1,25-dihydroxyvitamin D2 to lower or maintain lowered serum parathyroid hormone levels is disclosed. Dosage forms and dosing regimens are also disclosed.
US7550609 Biological conjugates for tumor targeted treatment; novel taxanes having mercapto or disulfide groups; side effect reduction without compromising their cytotoxicity A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.
WO2014159993A1 Triazine compounds and compositions thereof and methods for treating malaria and chemoprophylaxis Disclosed herein are triazine compounds and methods of making and using thereof to treat malaria, provide chemoprophylaxis, and/or treat or inhibit infection by one or more Plasmodium spp.
US20130074218 Method for optimising gene expression using synonymous codon optimisation The present invention discloses a method for modulating the quality of a selected phenotype that is displayed by an organism or part thereof and that results from the expression of a polypeptide-encoding polynucleotide by replacing at least one codon of that polynucleotide with a synonymous codon that has a higher or lower preference of usage by the organism or part thereof to produce the selected phenotype than the codon it replaces. The present invention is also directed to the use of a codon-modified polynucleotide so constructed for modulating the quality of a selected phenotype displayed by an organism or part thereof.
US20130030021 Substituted 2-(2,6-Dioxopiperidin-3-yl)-phthalimides and 1-Oxoisoindolines and Method of Reducing TNFalpha Levels Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines are disclosed. The compounds are useful, for example, in reducing the levels of TNFα in a mammal.
CN101214261B Medicament for mainly treating leukemia and preparation thereof The present invention relates to a drug which is mainly used for remedying leukaemia and is characterized by comprising the raw materials with the following weight portions of 75 to 150 portions of dog penises, 100 to 150 portions of black-striped snakes and 140 to 160 portions of chicken bones. The present invention also relates to a manufacturing method of the drug mainly remedying the leukaemia, which comprises the following steps that the black-striped snakes are processed for removing gall bladders, poison fangs and bowels to be cooked with the dog penises and the chicken bones in 500 to1000 portions of water; after being cooked, the marrow and the blood of the chicken bones, the dog penises and the black-striped snakes are taken out to be baked and dried to be made into powdery preparation. The present invention has the beneficial effects of good curative effect, convenient taking manner, simple manufacture and no toxic and side effect.
WO2006067867A8 Cell adhesion factor expression inhibitor A cell adhesion factor expression inhibitor comprising a proanthocyanidin, preferably a proanthocyanidin derived from pine bark. This inhibitor is obtained from plants and exerts an excellent cell adhesion factor expression effect.
CN101703486A Novel flutamide tablets and method for preparing same The invention discloses novel flutamide tablets. The main and auxiliary raw materials of each tablet comprise: 250mg of flutamide, 20 to 40mg of polyacrylic resin II, 15 to 30mg of polyacrylic resin III, 85 to 200mg of polyethylene glycol-6,000, 85 to 200mg of cross-linked polyethylene pyrrolidone, 40 to 125mg of microcrystalline cellulose, 3 to 5mg of miropowder silica gel and 500 to 2,500mg of medical ethanol; and the weight of each tablet is controlled within 500 to 850mg. The preparation method comprises the following steps of: firstly, preparing the particles of the flutamide and the polyacrylic resin, and mixing the particles with PVPP and the microcrystalline cellulose; secondly, placing the mixture in a boiling granulator; thirdly, injecting ethanol solution prepared by the PEG-6,000 and the flutamide in the boiling granulator to prepare particles in one step; and finally, finishing particles, adding a lubricant, totally mixing and pressing to obtain the flutamide tablets. The flutamide single-layer tablet can be quickly released and slowly released in a body at the same time in a quick release-slow release coexisting mode, and simultaneously the flutamide single-layer tablet also solves the problem of the dispersion and dissolution of the flutamide in gastric juice and intestinal juice.
CN1939315A Ganglioside solid lipid nano-particle of monosialic acid tetrahexose and its preparation A solid liposome nanoparticle of tetrahexose monosialogandlioside (GM1) is proportionally prepared from GM1, medicinal phosphatide, lipoid material and emulsifier. Said lipoid material is chosen from fatty acid, vegetative oil, glyceride of fatty acid, steroid and wax.
CN102038681A Medicinal composition for relieving cough and reducing phlegm The invention relates to a medicinal composition for relieving cough and reducing phlegm. The medicinal composition is prepared by mixing butamirate citrate, ambroxol hydrochloride and chlorphenamine maleate serving as active ingredients and pharmaceutical excipients. The composition can be prepared into oral preparations such as granules, tablets, capsules, oral liquid, syrup and the like. The medicinal composition can be used for treating related diseases such as cold and rhinitis with symptoms of cough, sputum, rhinobyon and rhinorrhoea and has obvious effect and high safety.
US7504437 Acetylcholinesterase inhibitor; Alzheimer's diseases, Hubtington disease, antidepressants A compound of the formula (I): wherein R1 represents C1–C6 alkyl, amino(C1–C6 alkyl)amino, di(C1–C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and represent hydrogen or C1–C6 alkyl; Ra represents C1–C6 alkyl or C2–C6 alkenyl or together with R2 represents a C1–C3 alkylene; Arom represents aryl or heteroaryl; A represents a C1–C6 alkylene; E represents a single bond, oxygen, sulfur or R4NR4—, wherein R4 is hydrogen or C1–C7 alkenoyl; X1 and X2 are the same or different and represent oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof. The compound has superior acetylcholinesterase inhibitory action and selective serotonin reuptake inhibitory action, and is useful for treating or preventing Alzheimer's disease, depression, Huntington's chorea, Pick's disease, tardive dyskinesia, compulsive disorders or panic disorders.
US20060111556 Preventives/remedies for neurodegenerative diseases A compound or its salts inhibiting the activity of the protein of the present invention, a compound inhibiting the expression of a gene for the protein, the antisense polynucleotide of the present invention, the antibody of the present invention, and the like can be used as prophylactic/therapeutic agents for neurodegenerative disease, diabetes and the like. A compound or its salts promoting the activity of the protein of the present invention, a compound promoting the expression of a gene for the protein, etc. can be used as prophylactic/therapeutic agents for cancer, rheumatic disease, etc.
WO2007095495A3 Benzodiazepine gcnf modulators for stem cell modulation A genus of benzodiazepines that modulate Germ Cell Nuclear Factor (GCNF) is disclosed. The compounds are useful to regulate stem cell differentiation and as contraceptives. Other embodiments are also disclosed.
US20080051324 Medium-Chain Length Fatty Alcohols as Stimulators of Hematopoiesis Medium-chain length fatty alcohols such as octanol, decanol, dodecanol, or analogues thereof can be used as a stimulator of hematopoiesis, hematopoietic stem cell proliferation, and/or proliferation of one or more of the progenitors of red or white blood cells (e.g., erythrocyte, leukocyte, neutrophil, granulocyte, megakaryocyte, or any combination thereof). It also relates to the treatment of myelosuppression; in particular, this includes the treatment of anemia and/or neutropenia associated with chemotherapy and/or radiotherapy. Moreover, anemia arising from chronic renal failure or treatment of HIV-infected patients with AZT (zidovudine), or other inhibitors of reverse transcriptase, can be treated. Furthermore, neutropenia arising from infections, hematologic diseases, or nutritional deficiencies can be treated. It also relates to reducing drug toxicity and enhancing drug efficiency.
WO2014049298A1 Combination of laropiprant and ivermectin for the treatment of rosacea The invention relates to a pharmaceutical composition, in particular a dermatological composition, comprising laropiprant, an ester or a pharmaceutically acceptable salt thereof and ivermectin or a pharmaceutically acceptable salt thereof, and to the use of same for the treatment of dermatological conditions, in particular rosacea.
CA2802334A1 Compositions and methods for imaging tissues, organs and tumors The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.
US7220425 Method for therapy of liver tumors A method for regional administration of preparations during the therapy of liver tumor, comprising administering a preparation into a branch of the portal vein with the simultaneous occlusion of afferent and efferent lobe vessels (branches of the portal vein proximal the place of puncture, branches of the hepatic artery and lobar hepatic vein) for 5–15 minutes. During catalytic therapy, it is preferable to use Teraphtalum as the preparation and to administer ascorbic acid after termination of occlusion. During photodynamic therapy, it is preferable to use photosens as the preparation and to carry out irradiation of the tumor after 10–35 minutes. This method of administration provides for the predominant accumulation of the preparations in the target lobe (tumor carrier lobe) of the liver, their low penetration into the systemic blood flow, which makes it possible to reduce the dose of the preparation and its general toxicity.
US8247403 Benzoxazepine derivatives and use thereof Compounds represented by the general formula (I): wherein each symbol is as defined in the description [with the proviso that 9-chloro-7-(1,1-dimethylethyl)-2,3,4,5-tetrahydro-1,4-benz-oxazepine and N-[[(5S)-2-oxo-3-(2,3,4,5-tetrahydro-1,4-benz-oxazepin-7-yl)-5-oxazolidinyl]methyl]acetamide are excluded], salts of the same, and prodrugs thereof have selective activation effect on serotonin 5-HT2C receptor and are useful as preventive and therapeutic agents for lower urinary tract diseases, obesity, and/or pelvic organ prolapse.
CN101273982A Medicament for preventing or/and treating depression The invention provides a medicine for prevention and/or treatment of depression, depressive state or anxiety neurosis, or a medicine for prevention and/or treatment of these diseases with a symptom of cerebrovascular obstacles; the medicine takes the substances selected from amino alkoxy bibenzyl compounds, pharmaceutical salts thereof, ester thereof, solvate and hydrate thereof represented by the formula (1) as effective ingredients, in the formula R<1> represents hydrogen atom, halogen atom, alkoxy including 1 to 5 carbon atoms, or dialkyl amino including 2 to 6 carbon atoms; R<2> represents hydrogen atom, halogen atom, alkoxy including 1 to 5 carbon atoms; R<3> represents hydrogen atom, hydroxyl, -O-(CH2)n-COOH (n represents an integer of 1 to 5) or -O-CO(CH2)l-COOH (l represents an integer of 1 to 3); R<4> represents -N(R<5>)(R<6>)(R<5> and R<6> each independently represents hydrogen atom or alkyl including 1 to 8 carbon atoms), m represents an integer of 0 to 5.
WO2007004912A1 Allergen The invention relates to the use of a birch bark extract for suppressing allergy.
US20120028912 Methods of modulating bromodomains The present invention features compounds useful for and methods for preventing or inhibiting the binding of bromodomains to acetyl-lysine residues of proteins and methods for treating HIV infection and HIV related disease.
CN1823872A Biological preparation capable of improving cardio cerebral function A biologic medicine for improving the functions of heart and brain is prepared from the yolk lecithin (20-80 Wt%) and rhodiola root (20-80 Wt%).
CN1600312A Combination of valaciclovir hydrochloride soft capsule A composite Wannailuowei hydrochloride in the form of liquid for preparing softgel contains Wannailuowei hydrochloride, solvent and surfactant.
WO2014129744A1 Four-membered cyclic nitrogen compound, pharmaceutical composition for preventing or treating depression, mental disorders, premature ejaculation or neuropathic pain, containing same, and preparation containing pharmaceutical composition The present invention relates to: a novel four-membered cyclic nitrogen compound capable of being used as an agent for treating or preventing depression, mental disorders, premature ejaculation or neuropathic pain by highly preventing the reabsorption of a specific neurotransmitter; a pharmaceutical composition capable of inhibiting the reabsorption of seretonin and dopamine or norepinephrine and having a high effect of treating or preventing depression, mental disorders, premature ejaculation or neuropathic pain; and a preparation containing the pharmaceutical composition.
WO2005032462A2 Glucocerebroside treatment of disease The present invention provides a method for the treatment of immune mediated or immune related diseases or disorders, infectious diseases, metabolic disorders and cancer in mammalian subjects. This method comprises the administration of a naturally occurring, mammalian intermediary metabolite or T cell receptor ligand, preferably a glucosylceramide, to a mammalian subject. In a preferred embodiment, such mammalian subjects are human beings.
WO2006115274A1 Myeloerythroid progenitor differentiation inducer It is intended to provide a myeloerythroid progenitor differentiation inducer comprising arginine as an active ingredient and a therapeutic agent for anemia comprising the differentiation inducer. The differentiation inducer is an excellent agent which is highly safe, can be orally administered and is widely used.
CN101439033A Polyenic taxusol lipid complexes and micelle composition thereof for injection The invention provides a docetaxel lipid compound and a micellar compound used in the injection of the docetaxel lipid compound, belonging to a pharmaceutical preparation. The docetaxel lipid compound is composed of docetaxel with a therapeutic dose, phospholipid, cholesterol sulfate or/and similar cholesterol derivative, additive and injection water. By means of the lipidization of the docetaxel, the problem about organic menstruum of an injection and the problem of hypersusceptibility of a surface active agent are solved. A docetaxel lipid compound injection provided by the invention has the advantages of small side effect, low blood vessel simulation, high drug-loading rate, narrow particle size distribution, capability of filtering and degerming, good pharmaceutical stability, etc.
WO2009134524A2 Method and system for the treatment of chronic obstructive pulmonary disease with nebulized anticholinergic administrations Inhalation solutions for administration of muscarinic antagonists for the treatment of breathing disorders, such as COPD, are provided.
CN101524331A Polysaccharide-liposome and preparation method and purpose thereof The invention relates to a polysaccharide-liposome which is prepared from raw materials such as polysaccharide, phosphatides, cholesterol, surface active agent and polyethyleneglycol. The liposome has smaller grain diameter and higher envelop rate. The invention particularly relates to a lentinan liposome and provides a preparation method of the polysaccharide-liposome and a purpose of the polysaccharide-liposome used for preparing drugs with the functions of antitumor or immunity adjustment.
US20060293351 Promotion of wound healing A promotor of wound healing and an inhibitor of formation of a urethral stricture, particularly following surgical intervention or infection in the area. Specifically, the most preferred compound of the present invention, Halofuginone, can be used to prevent collagen deposition from occurring within the lumen of the urethra after such trauma, thereby inhibiting urethral stricture formation. Halofuginone, and related compounds, are also useful for the promotion of wound healing after trauma, for example after surgery.
US8394824 Quinuclidine compounds having quaternary ammonium group, its preparation method and use as blocking agents of acetylcholine The invention relates to the quinuclidine compounds of formula I having quaternary ammonium group, its preparation, and the pharmaceutical composition comprising an effective amount of the compound of formula I. The compound and the composition are used to prevent and treat the diseases by blocking acetylcholine receptor. Wherein: R1 is selected from C1-12 saturated straight-chain alkyl and cycloalkyl; R2 is selected from C1-12 saturated straight-chain alkyl or straight-chain alkyl; and X is selected from halogen ion, organic and inorganic acid radical.
US20100317718 Modulation of hif1 beta expression Compounds, compositions and methods are provided for modulating the expression of HIF1-beta. The compositions comprise oligonucleotides, targeted to nucleic acid encoding HIF1-beta. Methods of using these compounds for modulation of HIF1-beta expression and for diagnosis and treatment of diseases and conditions associated with expression of HIF1-beta are provided.
US7429483 Use of nerve growth factor for the storage, culture or treatment of cornea The nerve growth factor (NGF) is used for the storage of corneas in culture, for the production and the storage in vitro of single cell populations of the corneal morphological and functional unit (i.e. epithelium, stroma/keratocytes and endothelium) and of the conjunctival epithelium, and for the production and the storage of corneal and conjunctival tissues, in particular for transplantation purposes. The NGF is also proposed for use in the therapy and/or the prophylaxis of diseases of the corneal surface, wherein a lack of integrity of the corneal and conjunctival morphological and functional unit occurs, in particular for pathologies having a dystrophic or neurodystrophic basis, both congenital and acquired.
WO2006042324A2 Antifungal composition applicable to body tissue, preferably nails The present invention provides a non-water soluble, film-forming composition which adheres to body tissue and forms a pharmaceutical carrier to provide localized delivery of an antifungal agent to a treatment site. The composition will typically include: (a) an alkyl cellulose; (b) a hydroxyalkyl cellulose; (c) a pharmaceutically acceptable polar protic solvent; (d) an antifungal agent selected from the group of naftifine, ciclopirox, terbinafine, pharmaceutically acceptable salts thereof, and combinations thereof; (e) an glycol ether; (f) an antipruritic agent selected from the group of camphor, menthol, butamben picrate, metacresol, benzyl alcohol, camphorated metacresol, juniper tar, phenol, phenolate sodium, resorcinol, camphorated metacresol, carbolic acid, and combinations,; and (g) a solubility enhancing agent, a surfactant, a wetting agent, or a combination thereof. The present invention also provides for the use of the composition composition of the present invention, in treating a fungal infection (e.g., nail fungus) in a mammal afflicted with such an infection.
CN102793713A Lincomycin hydrochloride-spectinomycin sulfate injection and preparation method thereof The invention provides a lincomycin hydrochloride-spectinomycin sulfate injection and a preparation method thereof. Water for injection is taken as a carrier; and 100ml of injection contains 3 to 7g of lincomycin hydrochloride and 8 to 12g of spectinomycin sulfate. The invention has the advantages that the injection is safe and reliable, and has low toxic or side effect and high bioavailability; lincomycin hydrochloride-spectinomycin sulfate is prepared into a compound hydro-acupuncture injection, the injection has a synergistic effect and a relatively wide antibacterial spectrum, can remarkably strengthen the antibacterial activity on mycoplasmas, can act quickly, and has low toxicity, and the therapeutic dose of the injection does not have adverse affect on chickens and pigs; and the injection has a good effect of treating respiratory diseases of livestock, particularly mycoplasmal pneumonia, digestive tract diseases of the livestock, and chicken chronic respiratory diseases which are caused by mycoplasma gallisepticums, is favorable for reducing the medicine tolerance of medicines, and prolongs the service life of the medicines.
US20100267841 Composition for Topical Use Containing an Extract of Stryphnodendron; Its Preparation As Well As Its Application The present invention relates to topical compositions containing extracts of the plant genus Stryphnodendron as well as their preparation and application. The compositions contain between 1% and 6% of total phenols and are useful for the treatment of cutaneous wounds.
CN101966149A Preparation of medicament fat emulsion for treating cerebral infarction The invention belongs to the field of medicine, relates to a medicinal injection preparation and a preparation method thereof, in particular to fat emulsion injection taking edaravone as an active ingredient and a preparation method thereof. The fat emulsion injection is prepared from the following components in percentage by weight: 0.1 to 4 percent of edaravone, 5 to 30 percent of oil for injection, 0.5 to 5 percent of emulsifier, 0.1 to 1 percent of active ingredient for inhibiting atherosclerosis, 0 to 5 percent of additive, and the balance of water for injection.
US8853216 Hydroxylated pyrimidyl cyclopentane as AKT protein kinase inhibitor The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.
CN101530610A Composition for cleaning liver and gall toxin Composition for cleaning liver and gall toxin comprises eatable composition A and composition B, wherein the composition A comprises coffee bean extract, panax japonicus extract, stachyose, palmitic acid, linoleic acid, wheat grass extract, tartaric acid, pectin, pineapple ferment and grape seed extract; and the composition B comprises coffee bean extract, panax japonicus extract, linolenic acid, lecithin, linoleic acid, stachys japonica extract, tartaric acid and pectin. The composition for cleaning liver and gall toxin can use physiological rhythm of the liver and gall to accumulate bile for increasing bile discharge pressure and promoting powerful contraction of the gallbladder, thereby cleaning metabolic waste in the liver and gall.
CA2440293C Catechins for the treatment of fibrillogenesis in alzheimer's disease, parkinson's disease, systemic aa amyloidosis, and other amyloid disorders A method of treating an amyloid disease, or a disease characterized by alpha-synuclein or NAC fibrillogenesis, in a mammalian subject. The method includes administering to the mammal a therapeutically effective amount of a various disclosed catechins or green tea extract. A pharmaceutical composition comprising a therapeutically effective amount of a catechin and pharmaceutically acceptable excipient. The therapeutic amount of the catechin or green tea extracts is selected for efficacy in treating amyloid, alpha-synuclein or NAC fibrillogenesis in a mammalian subject.
CN101074271A Production and use for amphipathic chitose derivative Production of amphiphilic chitose derivative and its usage are disclosed. The process is carried out by taking chitose as raw material, alkalizing, reacting with 4-methyl bromoethyl acid in 2-propanol medium to obtain 6-0-carboxy-propyl-chitose, purifying, and reacting with long-chain fatty acyl chloride to obtain N-acyl-6-0-carboxy-propyl-chitose. In chemical formula, R=-(CH) n, n=8, 10, 12, 14, 16 and 18. It has excellent biological compatibility and degradation, good tissue adhesion and mechanical strength. It can improve wound heal and have styptic and adhesion-preventing functions.
WO2007003941A1 Modulation of autophagy by calpain inhibition The present invention relates to finding that the inhibition of calpain induces autophagy in eukaryotic cells through an mTOR independent pathway. Methods and materials are provided for the treatment of diseases which are ameliorated by the induction of autophagy by inhibiting calpain such as neurodegenerative and infections diseases . Also provided are screening methods for identifying compounds which inhibit calpain and may be useful for treating such conditions .
US20050187179 treatment of tumors which have increased Notch expression; administration of either Notch antisense oligonucleotides or monoclonal antibodies directed to Notch along with cell differentiating agent Methods and compositions are disclosed for inducing differentiation and apoptosis in cells that overexpress Notch proteins. A cell fate determining function of Notch is specifically disrupted at a time when the cell is undergoing differentiation, which causes the cell to undergo apoptosis. The invention includes therapies for tumors that overexpress a Notch protein (such as Notch-1) by inducing differentiation of the cells in the tumor with a differentiation inducing agent, such as HMBA, in combination with an agent that disrupts the function of the Notch protein. At a time during which differentiation has been promoted, and the cell is susceptible to interference with the anti-apoptosis effect of Notch, the function of the Notch protein is disrupted. Disruption of Notch function can be achieved, for example, by a differentiation inducing agent, such as HMBA, combined with antibodies that specifically bind to Notch and inactivate it, for example a monoclonal antibody that recognizes Notch-1 EGF-like repeats 11 and 12, such as monoclonal antibodies A6, C11 or F3. Disruption of Notch function can also be achieved by the expression of antisense oligonucleotides that specifically interfere with expression of the Notch protein on the cell, alone or in combination with antineoplastic agents.
CN103585135A Application of magnolol to preparation of medicine for treating cachexia and cancer The invention discloses applications of magnolol, or isomers of magnolol or salts of compounds that are acceptable in pharmaceutical areas to preparation of medicines for treating cachexia and cancers. The cachexia may be caused by selection of the following groups of diseases, states or damage: cancers, immunodeficiency diseases, infectious diseases, autoimmune diseases, metabolic diseases, chronic bowel, liver, kidney, lung and heart diseases, anorexia nervosa, trauma, burning, malabsorption and anemia. In one embodiment, the medicines can be taken by patients that may suffer from cachexia such as cancers. The invention also provides applications of magnolol, or isomers of magnolol or salts of compounds that are acceptable in pharmaceutical areas to preparation of medicines for treating bladder cancers, especially applications to prevention of tumor growth and cancel cell metastasis of bladder cancers and to improvements of animal survival rates.
CN101987093A Ferrous lactate gel skeleton slow-release preparation and preparation method thereof The invention discloses a ferrous lactate medicine composition for oral administration. The ferrous lactate medicine composition is a gel skeleton slow-release preparation, and the gel skeleton is made of a slow-releasing material. The ferrous lactate medicine composition comprises the following components in dry weight: 100 parts of ferrous lactate, 40-120 parts of slow-releasing material and 1-20 parts of binding agent, wherein the slow-releasing material is selected from hydroxypropyl methyl cellulose and/or ethyl cellulose, and the binding agent is selected from polyvinylpyrrolidone, disaccharide, polysaccharide, an ethanol solution or a mixture thereof. The slow-release preparation conforms to the rules of pharmacopeia, reduces medicine taking times, stabilizes blood concentration, reduces the stimulation on the gastrointestinal tract and simultaneously increases the obedience of patients.
CA2428015C Process for the rehydration of magaldrate powder The present invention relates to a novel process for the rehydration of magaldrate powder by mechanical processing of aqueous suspensions of magaldrate powder.
EP1453806B1 Aminotetralin derivatives as muscarinic receptor antagonist This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by the general formula (I) wherein R?1, R2, R3 and R4¿ are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, processes for their preparation and their use as therapeutic agents.
CN101896473B Inhibitors of stearoyl-coa desaturase Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity.
US20120302816 Therapeutic compositions and methods for targeted delivery of active agents The present invention pertains to therapeutic compositions that comprise: (1) a nanovector, (2) an active agent; and (3) a targeting agent, wherein the active agent and the targeting agent are non-covalently associated with the nanovector. The present invention also pertains to methods of treating various conditions in a subject by utilizing the above-described therapeutic compositions. Methods of making the therapeutic compositions are also a subject matter the present invention.
EP1372383B1 A product comprising a susbtrate and an antimicrobial formulation Antimicrobial formulations, which may be essentially free of an antimicrobial active, comprising one or more proton donating agents and an alkyl phosphate anionic surfactant comprising a mono alkyl phosphate having the chemical structure: (I),wherein is a saturated or unsaturated straight chain or branched alkyl group having from about 8 to about 22 carbon atoms, x is a number from 0 to about 20, and and are independently selected from hydrogen, an alkali metal, or an alkanol amine, are provided and described herein. The formulations may be incorporated into wet wipes or various other personal care items such as facial tissue, bathroom tissue or feminine care products, or may be incorporated into lotions or soaps which may be applied directly to the skin. The antimicrobial formulations of the present invention have been found to have surprisingly high activity against numerous bacteria and other micoorganisms.
WO2007042910A1 Imidazoles and their use as hmg-coa reductase inhibitors Novel imidazole compounds of formula (I) and pharmaceutical compositions are described, as are methods of using such compounds, alone or in combination with another pharmaceutically active agent, to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and atherosclerosis.
EP1940781A1 Phenyl-acetamide nnrt inhibitors The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1-R4 and Ar are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
WO2008080988A3 Cyclopentanone derivatives, method of synthesis and uses thereof The present invention relates to cyclopentanone derivatives of formula (I), their method of synthesis and uses thereof. Also, the present invention relates to the use of cyclopentanone derivatives of formula (Ia). Concretely, the compounds disclosed have proved to be inhibitors of glycogen synthase kinase 3β, GSK-3 β, which is known to be involved in different disease and conditions, such as Alzheimer's disease or non-insulin dependent diabetes mellitus. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a GSK-3 mediated disease or condition.
US20080249107 Comprising trihydroxy phenyl subunits; selectin inhibitors; side effect reduction; 3-{3-[3-(3,4,5-Trihydroxy-phenyl)-propionylamino]-phenylamino}-benzoic acid Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols, indices and substituents have the following meaning R1═H, CN, NO2, CF3, F, Cl, Br, I, CH3 R2═H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl and either R1 or R2 must be H R3═H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl then X is e.g. with R4 being H, CH3, CH2CH3 or and Y being or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds of formulas (Ia) or (Ib). The compounds are applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
WO2007124642A1 A pharmaceutical formulation for treating tinea of feet and hands and preparation thereof A pharmaceutical formulation made from Fructus Gleditsia, Alumen and Borneol for treating tinea of feet and hands is disclosed. Also disclosed is a process of preparation of the pharmaceutical formulation, which comprising Fructus Gleditsia is decocted with water, and the decocted liquid is dried under reduced pressure to form the fine powder which is formulated to a cream together with the fine powders of Alumen and Borneol as well as the respective excipients.
CN101716186B Wound antibiotic flushing fluid and preparation method thereof The invention discloses a wound antibiotic flushing fluid and a preparation method thereof. Counted by 100 ml of wound antibiotic flushing fluid, the formula of the wound antibiotic flushing fluid comprises the following raw materials: 0.01-2 g of chlorhexidine salt, 3-1,000 micrograms of silver nitrate, 10-70ml of absolute ethyl alcohol, 5-20 ml of emollient, 0.5-5g of thickening agent, 0.05-5g of polysorbate 80, 0.5-5g of PH adjusting agent and 20-90ml of deonized water, wherein the chlorhexidine salt is chlorhexidine acetate or chlorhexidine gluconate; and the emollient is glycerol. The preparation method comprises the following steps of: dissolving the thickening agent in the deonized water, then respectively adding the chlorhexidine salt, the silver nitrate, the absolute ethyl alcohol,the emollient, the tween 80 and the PH adjusting agent into the mixed solution and stirring for 30 minutes to 2 hours. The wound antibiotic flushing fluid contains various antibiotic components and considerably strong broad spectrum bacteriostasis and sterilization functions, can kill various bacterial and fungus and has constant antibacterial action.
US20080289065 Peptide Aptamers That Bind to the Rep Proteins of Ssdna Viruses Polypeptides and fusion proteins that bind to eukaryotic viruses, in particular, eukaryotic single-stranded DNA (ssDNA) viruses are provided. The polypeptides and fusion proteins bind to the replication initiation proteins (Rep) of ssDNA viruses and optionally inhibit viral replication and/or viral infection. The virus can be a plant pathogen or animal pathogen. Consensus sequences used to identify polypeptides that bind to eukaryotic viruses are also provided.
US20090317471 matrix contains drug (hypotensive agents, antidepressants, anticonvulsants), ionic non-gelling matrix polymer (cellulose acetetate phthalate), and pH modifier; free of gelling or swelling excipient The present invention includes a controlled-release composition having a matrix. The matrix contains a pharmaceutically effective amount of an active agent or a pharmaceutically acceptable salt or solvate thereof, an ionic non-gelling matrix polymer, and a pH modifier. The ionic non-gelling matrix polymer is practically insoluble and unswellable at a first aqueous fluid pH and is soluble at a second aqueous fluid pH. The pH modifier is present in an amount to control the release of the active agent from the composition. The controlled-release composition is substantially free of a gelling or swellable excipient and does not contain a functional coating or a lipophilic component. The present invention also provides methods of making and using the controlled-release compositions.
CN103083331A Application of solanum laciniatum ketene in preparing antitumor medicines The invention belongs to the fields of chemical engineering and medicines, and relates to the application of solanum laciniatum ketene in preparing antitumor medicines. The invention provides the application of solanum laciniatum ketene in preparing antitumor medicines. The tumor cells comprise liver cancer cells, blood cancer cells, cervical cancer cells, breast cancer cells, and pancreatic cancer cells. Solanum laciniatum ketene is a natural product with low toxic and side effect, high bioavailability, stable quality, and clinical application values. The small-molecular compound provided by the invention is developed as a novel antitumor medicine or an auxiliary component thereof. A tumor inhibiting effect is substantial, and the compound is green and environment-friendly. Therefore, novel approach and means are provided for treating and curing tumors.
US8119163 Nanoparticulate and controlled release compositions comprising cefditoren The present invention provides a composition comprising a cefditoren, or a salt, derivative, prodrug, or other form thereof, for example, cefditoren pivoxil, useful in the treatment and prevention of infections and related conditions. The invention provides a composition which comprises nanoparticulate particles comprising the cefditoren, or a salt, derivative, prodrug, or other form thereof and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. The invention provides also a composition that delivers a cefditoren, or a salt, derivative, prodrug, or other form thereof, or nanoparticles comprising the same, in a pulsatile or continuous manner.
WO2014154025A1 Application of a flavonoid in pharmaceutical preparation The present invention discloses the application of a flavonoid in the preparation of a pharmaceutical for synthesizing and releasing an agent for inhibiting leukocyte inflammation, inhibiting at the origin the generation and release of inflammatory factors caused by microorganisms or chemical stimuli, and promoting leukocyte generation and releasing pro-resolving mediators in order to relieve inflammation.
WO2011163430A1 Polymorphs of osi-906 Polymorphic forms of the tyrosine kinase inhibitor OSI-906, preparation, pharmaceutical compositions, and uses thereof. The invention includes methods of treating diseases such as cancer, including cancer mediated at least in part by IGF-1 R and/or IR, with the polymorphs and compositions. This Abstract is not limiting of the invention.
WO2012138846A3 Method and compositions comprising small rna agonist and antagonists to modulate inflammation The disclosure provides methods and compositions for modulating inflammation.
US20080108706 dosage forms contains N1,N14-Diethyl-3(R) 12(R)-dihydroxyhomospermine for TREATMENT OF PANCREATIC CANCER A method of chemically resecting the exocrine portion of the pancreas of a patient in need thereof comprising administering to the patient an amount of a hydroxy polyamine or a salt thereof with a pharmaceutically acceptable acid sufficient to resect the exocrine portion of the pancreas thereof, but insufficient to substantially alter the endocrine portion thereof. The hydroxy polyamine has a structure according to the formula: wherein: R1 and R2 may be the same or different and are alkyl having 1 to 6 carbon atoms or aryl or aralkyl having up to 12 carbon atoms; a, b, d and e may be the same or different and are integers from 1 to 4; and c is an integer from 2 to 6. A pharmaceutical composition in unit dosage form comprising the hydroxy polyamine or a salt thereof with a pharmaceutically acceptable acid for use in the method of the invention is also disclosed.
EP2172198A1 p27 PROTEIN INDUCER The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from -N= etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from -CH2- etc., and R2 is selected from C1-6 alkyl etc.
CN103288916A Derivatives of tanshinone compounds as well as synthesis method and application thereof The invention discloses a derivative of a tanshinone compound as well as a synthesis method and application thereof. The derivatives of the tanshinone compounds have a structure of formula (I) or (II) shown in the specification, wherein R1 is CH3 or CH2OH; R2 is CH3 or CH2OH; R3 is L-amino acid or C1-C3 alcohol-esterified L-amino acid. According to the experiments, the derivatives of the tanshinone compounds disclosed by the invention have an obvious cytotoxic effect for tumor cells; according to the clone formation assay, the derivative disclosed by the invention has certain radio-sensitization, and has good prospect when used as an anti-tumor drug.
US20080242651 3-(2-cyclopentyl-2-phenyl-2-hydroxyacetoxy)-1-(carboxymethyl)-1-methylpyrrolidinium inner salt; muscarinic receptor antagonist; chronic obstructive pulmonary disease or asthma; synergistic mixture with antiinflammatory corticosteroid, betamimetic agent or antiallergic agent Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
WO2007003521A3 Pyridazine derivatives as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions, as 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) inhibitors.
WO2012059932A1 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.
WO2013117504A1 Pi3k inhibitors for treating cough The present invention is directed to compounds or pharmaceutically acceptable salts thereof for use in the treatment of cough, in particular idiopathic chronic cough, cough variant asthma, cough associated with thoracic tumour or lung cancer, viral and post-viral cough, upper airways cough syndrome (UACS) or post nasal drip cough, and cough associated with disorders such as gastro oesophageal reflux disease (both acid and non acid reflux), chronic bronchitis, chronic obstructive pulmonary disease (COPD), interstitial lung disease (such as idiopathic pulmonary fibrosis (IPF)), congestive heart disease, sarcoidosis and infection (such as whooping cough).
US7034005 Use of macrolide derivatives such as 6,15,16-Trioxatricyclo(10.2.1.11,4) hexadecane, erythromycin derivative The present invention relates to agent for suppressing infection and proliferation of human immunodeficiency syndrome virus (HIV-1), which infects immunocompetent cells such as macrophage or dendritic cell and causes destruction of immune system, and use of known compounds, macrolide derivatives for suppression of infection and proliferation of human immunodeficiency syndrome virus in M type macrophage derived from human monocytes. The present invention is useful for treatment of patients with HIV-1 infection by low cost chemotherapeutic agents, and in addition, is clinically used as supplement agent in HAART.
CN1861045A Coenzyme Q10 venoclysis injection A coenzyme Q10 injection with high optical stability for intravenous injection contains coenzyme Q10, solubilizer, solvent for injection and osmotic pressure regulator.
US20060189663 Pyrrole-2,5-dithione derivatives as liver x receptor modulators The present invention relates to certain novel compounds of the Formula I to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
US7709445 Colloidal suspension of nanoparticles based on an amphiphilic copolymer An aqueous suspension, stable in physiological medium, of nanoparticles for delivering active principles such as insulin. The delivery particles are based on a three-block copolymer: polyethylene glycol/hydrophilic polyaminoacid/hydrophobic polyaminoacid. These three-block copolymers can be associated with an active principle without denaturing it, and perform a controlled and long-term release of the active principle in vivo, and thus provide the active principle with a very prolonged release. Also disclosed is a powder form solid from which are derived the delivery particles, the preparation of the powder-form solid, a suspension of delivery particles based on the three-block copolymer, and pharmaceutical specialties obtainable from the delivery particles filled with active principle.
CN103211789A Ambroxol hydrochloride film-controlled slow-release pellet capsule The invention relates to an ambroxol hydrochloride film-controlled slow-release pellet capsule. A slow-release film of the ambroxol hydrochloride film-controlled slow-release pellet utilizes Kollicoat SR 30D as a film-formation material. A pellet core of the ambroxol hydrochloride film-controlled slow-release pellet contains low-substituted hydroxyprepyl cellulose having high expansibility, and also contains pharmaceutically-acceptable common excipients for the slow-release pellet, wherein preferably, the excipients comprise microcrystalline cellulose and lactose, and the pellet core comprises 10 to 40wt% of low-substituted hydroxyprepyl cellulose. The slow-release film comprises Kollicoat SR 30D, triethyl citrate as a plasticizer, and talcum powder as an antiplastering aid, wherein preferably, a ratio of Kollicoat SR 30D to triethyl citrate to talcum powder is 30: 1.5: 4 and a film weight increasing ratio is in a range of 20 to 36%. The ambroxol hydrochloride film-controlled slow-release pellet comprises the pellet core containing low-substituted hydroxyprepyl cellulose having high water expansibility and thus after absorbing water, the ambroxol hydrochloride film-controlled slow-release pellet obviously expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the ambroxol hydrochloride film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.
WO2012101068A1 Novel tetrahydroquinoline derivatives A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein R1 to R8, A1 to A3 have the significance given in claim 1, can be used as AMPK modulators for treating obesity, hyperglycemia or type 2 diabetes.
US20100010229 Fexofenadine polymorph The present invention provides a novel fexofenadine hydrochloride polymorph. The polymorph is particularly useful as a medicament for use as an antihistamine, antiallergy agent or bronchodilator.
US20090111763 Loadable polymeric particles for bone augmentation and methods of preparing and using the same Particles are provided for use in therapeutic and/or diagnostic procedures. The particles include poly[bis(trifluoroethoxy)phosphazene] and/or a derivatives thereof which may be present throughout the particles or within an outer coating of the particles. The particles may also include a core having a hydrogel formed from an acrylic-based polymer. Such particles may be provided for placement within defects in bone within the body of a mammal to augment structural support and facilitate osteogenesis without causing adverse reactions therein. The hydrogel core may further be used as a delivery vehicle for therapeutic agents to treat or retard pathologic processes within the bone defect during healing.
US20100008868 Sustained remission of atopic dermatitis It has been found that the combination of an antihistamine with a corticosteroid is more effective in the treatment of atopic dermatitis than either one used separately. The synergistic effect in some cases results in the disappearance of the atopic dermatitis lesion within one to five days with little or no relapse. Compositions and the methods of utilizing these preparations are disclosed.
EP2351749A1 Carbamate compound or salt thereof [Problems] A compound useful as an active ingredient for a pharmaceutical composition for treating FAAH-related diseases is provided. [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that a piperazine-1-carboxylate compound, in which benzimidazol-2-ylcarbonyl, benzofuran-2-ylcarbonyl or the like binds to the 4-position of the piperazine, has an excellent FAAH inhibitory activity and further has an action to increase the effective bladder capacity, an action to ameliorate sleep disorders, an anti-diuretic action, and an analgesic activity on lower urinary tract pain including bladder pain and the like, thereby completed the present invention. The carbamate compound of the present invention has an excellent FAAH inhibitory activity and can be used as an agent for preventing and/or treating FAAH-related diseases, particularly nocturia, interstitial cystitis, painful bladder syndrome, or chronic non-bacterial prostatitis/chronic pelvic pain syndrome.
WO2005096692A3 Crystalline forms of mizolastine, production methods thereof and pharmaceutical compositions containing same The invention relates to a crystalline form mizolastine which is substantially free of water and solvent and which is known as Form A and another crystalline form of mizolastine which is substantially free of solvent and which is known as Form B, said two forms being characterised by infrared spectroscopy, differential scanning calorimetry and X-ray powder diffraction. The aforementioned crystalline forms can be obtained by means of recrystallisation of mizolastine in an organic solvent in the presence or absence of water. The pharmaceutical compositions containing said crystalline forms can be used for the treatment of allergic disorders.
CN102603396A Preparation of chitosamine-selenium nanometer trace-element nutrition regulator The invention relates to a preparation method of a nanometer chitosamine-selenium preparation. The method comprises the steps of: dissolving sodium selenite in an ethanol solution of which the mass fraction is 75% to prepare a sodium selenite solution of which the mass fraction is 12.5%; weighing chitosamine and dissolving in distilled water to prepare a chitosamine solution of which the mass fraction is 8%; mixing 50ml of chitosamine solution with 40ml of sodium selenite solution, adding 10mg of surfactant and magnetically stirring for 30minutes; and carrying out pulsed ultrasound for 15minutes at a room temperature to obtain a chitosamine-selenium nanometer microsphere turbid liquid which is subjected to crosslinking and uniformly dispersion. The preparation method of a plant growth regulator chitosamine-selenium nanometer trace-element nutrition regulator is simple to operate, low in cost, easy in reaction control and high in product quality, and has no pollution; and the prepared nanometer preparation can be used for regulation of agricultural plant growth.
US20100099754 5,6-dimethyl xanthone-4-acetic acid derivatives and method of preparing the same A method of preparation of 5,6-dimethylxanthone-4-acetic acid (DMXAA) and derivatives thereof. The derivatives are represented by formula (I), wherein R represents totally 1 to 2 substitutes at 1, 2, 3, 7, and 8 position selected from a lower alkyl, halogen, CF3, CN, NO2, NH2, CH2COOH, OR2, OH, NHSO2R2, SR2, CH2CONHR2 or NHR2, and R2 represents a lower alkyl, or a lower alkyl having OH, NH2, or OCH3. The invention further provides a pharmaceutical composition having such derivatives used as excellent antitumor and antibacterial agents.
WO2009031318A1 Preparation for external application comprising analgesic/anti-inflammatory agent Disclosed is a preparation for external application, which comprises the following components (A) and (B): (A) a non-steroidal analgesic/anti-inflammatory agent; and (B) a polyoxyalkylene alkyl ether and/or a polyoxyalkylene alkenyl ether. The preparation for external application is improved in the skin permeability of the non-steroidal analgesic/anti-inflammatory agent and therefore can exhibit the efficacy of the non-steroidal analgesic/anti-inflammatory agent at a low concentration, and has excellent appearance.
EP1844772A1 Compositions for transfection of oligonucleotides active for gene silencing and their biological and therapeutical applications The invention relates the compositions of transfection comprising an oligonucleotide active for RNA interference and an amphiphilic cationic molecule of formula (I) wherein - X is N-R1, S or 0, R1 being a C1-C4 alkyl radical or an hydroxylated C3- C6 alkyl radical, - R2 and R3, identical or different, represent H or a C1-C4 alkyl radical, or R2 and R3 are linked together to form a cycle or a heterocycle having 6 elements, - E is a C1-C5 alkyl spacer, - R4 and R5, identical or different, represent saturated or unsaturated, linear or branched, C10-C36 hydrocarbon or fluorocarbon chains, optionally comprising C3-C6 cycloalkyle, - A- is a biocompatible anion. Use of said compositions as drugs.
US20090023748 Cysteine Protease Inhibitors Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl- moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
US20060142396 Use of GABA agonists for the treatment of spastic disorders, convulsions, epilepsy, and neuroprotection A method of treating a neuronal disorder is provided that includes the intravenous administration to a subject suffering or predisposed to a neuronal disorder a therapeutically effective amount of gamma-aminobutyramide or a pharmaceutically acceptable salt thereof. Gamma-aminobutyramide has sufficient stability for intravenous administration and is able to cross the blood-brain barrier. A method of neuroprotection is provided that includes administration to a subject suffering or predisposed to a neuronal disorder associated with spasticity or convulsions a therapeutically effective amount of gamma-aminobutyramide or a pharmaceutically acceptable salt thereof.
CN101252938A Combined preparation of a thiazide diuretic and a loop diuretic The invention relates to pharmaceutical preparations which contain a combination of a thiazide diuretic and a low dose of a loop diuretic and which is particularly suitable for treating hypertension and heart failure. It is not only the natriuretic/diuretic effects which are increased due to said combination of thiazide diuretic and loop diuretic, but also the undesired secondary effects in relation to potassium and magnesium losses are also significantly reduced. As a result, the desired hypocalciuric effect of the thiazide is maintained despite the presence of the loop diuretic.
US20120107407 Bone graft and biocomposite for prosthetic dentistry A bone graft or biocomposite for treating osseous defects and neogenesis of bone which is a composite of a biodegradable polymer and granules of beta-tricalciumphosphate, further comprising as active ingredient and embedded in the biodegradable polymer a physiologically effective amount of underglycosylated recombinant human BSP as a muti-dental clathrate with a basic organic compound which simulataneously is active as a plasticizer for the biodegradable polymer. The biocomposite is moldable and shapeable, hardens rapidly in situ when placed by surgery or prosthetic dentistry and which furthers osseous repair and the healing of damage or diseased tissues and lesions.
CN201578615U Microgranular texture The utility model provides a microgranular texture, in particular to a microgranular texture comprising film coating, which comprises a core part and an outer film coating; the core part is a structure mixed by carbon powder and adhesive; the film coating is coated on the core part to form a microgranular texture provided with the film coating; and the microgranular texture takes the different pH values of each part of a gastrointestinal tract as the controlled release condition; wherein the film coating begins being dissolved when the pH value is 5.5; when the pH value reaches 7.0, the outer film coat is completely dissolved so as to collapse the carbon powder of the core part to play the most complete poison absorption effect so as to improve the defects that oral carbon products are mostly and instantly collapsed when being centralized in a stomach and can not absorb the piston at large intestine after collapse.
WO2008012932A1 Insulin resistance reducer As one example of investigating effects of accumulation of chondroitin sulfate proteoglycan (CSPG), the invention relates to a versican siRNA containing a core site sequence of versican which is one of the chondroitin sulfate proteoglycans, an siRNA of C4ST1, C4ST2 or C4ST3 which is an enzyme transferring a sulfate group of acetylgalactosamine being a side chain of chondroitin sulfate proteoglycan, and an insulin resistance reducer suitable for gene therapy or prevention for a disease caused by an increase in insulin resistance such as type II diabetes (NIDDM). The invention also relates to a method of reducing insulin resistance based on inhibiting the accumulation of chondroitin sulfate proteoglycan (CSPG) by administering a versican siRNA, C4ST-1 siRNA, C4ST-2 siRNA or C4ST-3 siRNA to a test subject and a method of treating or preventing a disease caused by an increase in insulin resistance such as type II diabetes utilizing the same.
CN1762365A Beta-carotene clathrate and its preparation method The invention provides a beta-carotene inclusion compound, which comprises beta-carotene and beta-cyclodextrin derivative by the weight ratio of 1:9-50. The preparing process comprises the steps of mixing beta-cyclodextrin derivative with beta-carotene, grinding 1-3 hours, dissolving with right amount of alcohol, agitating, evaporating the dissolvent and dissolving the solid inclusion compound into water, stewing 12-24 hours at a low temperature, decompression concentration, vacuum drying 3-6 hours at 35-50 deg C.
US20120322892 Oral microemulsion of elemene An oral microemulsion of elemene is disclosed. The microemulsion is made of elemene, surfactant, cosurfactant and water or buffer solutions with pH 5˜8. Said surfactant is selected form tweens, polyoxyethylene castor oils, polyethylene glycol stearates and mixture thereof. Said cosurfactant is selected from ethanol, 1,3-propanediol, glycerol and mixture thereof. The concentration of elemene in the microemulsion is 1˜5 g/100 ml. The ratio of elemene, surfactant and cosurfactant is 1˜5(weight):1˜40(weight):1˜40(volume), wherein the unit of weight/volume is g/ml.
EP1749527A1 Use of substituted pyrazoline compounds for the treatment of the lipid parameters of the metabolic syndrome The present invention relates to the use of substituted pyrazoline compounds for the treatment of the lipid parameters of the metabolic syndrome in humans and animals.
US20100178258 Composition and method for the treatement of skin irritations A composition is provided that is suitable for topical administration for the treatment of a skin irritation, the composition comprising acetylsalicylic acid and sodium bicarbonate. Also provided is a method for treating a skin irritation in an individual comprising topically administering to the affected area a therapeutically effective amount of a composition comprising acetylsalicylic acid and sodium bicarbonate. The composition is particularly useful for decreasing the temperature at the surface of a sunburn and for reducing pain and discomfort caused by a sunburn.
WO2012026495A1 Novel hydantoin derivative and medicinal agent comprising same as active ingredient The present invention provides a compound which has a potent AMPK activation activity and exhibits an advantageous effect that comes from the AMPK activation activity in vivo. The present invention relates to a hydantoin derivative represented by general formula (1), a pharmacologically acceptable salt of the derivative or a hydrate of the derivative or the pharmacologically acceptable salt.
US20080214669 Hydroxycinnamic acid, a methoxycinnamic acid, dissolved in a compound having hydroxy groups; lightening skin An improved cosmetic and dermatological composition and a method for treating hyperpigmented skin is disclosed. The composition demonstrates an enhanced ability to lighten mammalian skin color, and is nontoxic and nonirritating. The composition comprises a hydroxycinnamic acid or a methoxycinnamic acid dissolved in a compound having one or more hydroxy groups, like a monoC1-4alkyl ether of an ethylene glycol or a monoC1-4alkyl ether of a propylene glycol oligomer, and/or a silicone fluid.
US7056524 Methods of hydrating mucosal surfaces A method of hydrating nasal airway surfaces in a subject in need of such treatment comprises topically applying a sodium channel blocker to a nasal airway surface of the subject in an amount effective to inhibit the reabsorption of water by the surface. The channel blocker may be a pyrazinoylguanidine sodium channel blocker, such as benzamil, phenamil, amiloride, or a pharmaceutically acceptable salts thereof. The method may further comprise the step of topically applying a P2Y2 receptor agonist to a nasal airway surface of the subject in an amount effective to stimulate chloride secretion by the nasal airway surface. In a preferred embodiment, the sodium channel blocker is a covalent conjugate of a pyrazinoylguanidine sodium channel blocker and a non-absorbable carrier moiety (e.g., albumin, polyethylene glycol). Such compounds may also be administered to other mucosal surfaces where it is desired to inhibit the reabsorption of water.
US20090118249 Dheas inhalation compositions The present invention provides compositions for aqueous suspension comprising DHEAS and a divalent cation. The suspension in combination with a nebulizer or nasal pump spray can be administers as an aerosol for the treatment of respiratory diseases and conditions. The present invention also provides methods for making compositions in form of aqueous suspension of DHEA and divalent cations.
US20110110884 Immunotherapy for immune suppressed patients The present invention provides compositions of a natural cytokine mixture (NCM) for treating a cellular immunodeficiency characterized by T lymphocytopenia, one or more dendritic cell functional defects such as those associated with lymph node sinus histiocytosis, and/or one or more monocyte functional defects such as those associated with a negative skin test to NCM. The invention includes methods of treating these cellular immunodeficiencies using the NCM of the invention. The compositions and methods are useful in the treatment of diseases associated with cellular immunodeficiencies such as cancer. Also provided are compositions and methods for reversing tumor-induced immune suppression comprising a chemical inhibitor and a non-steroidal anti-inflammatory drug (NSAID). The invention also provides a diagnostic skin test comprising NCM for predicting treatment outcome in cancer patients.
CN102295654B Cefoxitin compound and composition thereof The invention relates to a cefoxitin compound. The cefoxitin compound is determined by the method of powder X-ray diffractometry, and characteristic diffraction peaks appear at 5.8 degrees, 7.4 degrees, 8.6 degrees, 13.0 degrees, 14.8 degrees, 15.2 degrees, 16.5 degrees, 18.7 degrees, 23.1 degrees and 25.2 degrees in an X-ray powder diffraction spectrum which is represented by the angle of diffraction 2theta plus or minus 0.2 degree. The invention also relates to a composition of the cefoxitin compound, and the composition comprises 90 to 100 parts of the cefoxitin compound and 0 to 2000 parts of a pharmaceutically acceptable carrier, preferably 0.1 part to 1000 parts of the pharmaceutically acceptable carrier, more preferably 1 part to 500 parts, and most preferably 1 part to 5 parts.
WO2012103777A1 Compound isolated from monascus purpureus, preparation method therefor and uses thereof Disclosed is a compound isolated from monascus purpureus, a preparation method therefor and uses thereof. Specifically, the compound is as represented in formula I, or pharmaceutically acceptable salts thereof, where R1 is selected from hydrogen, hydroxyl group, C1-6 straight-chain or branched-chain alkoxy group, [formula II], [formula III] and [formula IV]; R2 is hydrogen or alkyl group; R3 is selected from hydrogen, hydroxyl group, C1-6 straight-chain or branched-chain alkoxy group. Also disclosed in the present invention is a pharmaceutical composition containing the compound. The compound of the present invention has an inhibitive effect on HMG-CoA reductase. Formula I.
WO2007144152A2 Extended step-down estrogen regimen The present invention relates to methods for treating diseases, conditions or symptoms associated with deficient endogenous levels of estrogen comprising administration of a higher first dose of an estrogen followed by administration of a lower second dose of an estrogen once therapy has been effectively established. The invention further relates to a combination treatment comprising administration of an estrogen and a progestin.
EP1265920B1 Angiogenesis-associated proteins, and nucleic acids encoding the same An isolated polypeptide having at least 80 % sequence identity to the sequence SEQ ID NOS: 2, 4, 6, 8, 10, 12, 14 or 16, and polynucleotides encoding the same, are useful for modulating angiogenesis.
US20110039908 Inhibiting Amyloid-Beta Peptide/Rage Interaction At The Blood-Brain Barrier Small molecules are used to inhibit specific receptor-ligand interaction between Alzheimer's amyloid-β peptide (Aβ) and Receptor for Advanced Gly-cation Endproducts (RAGE). Objectives include treating Alzheimer's disease and other pathologies involving cerebral amyloid angiopathy; improving blood flow to or within the brain; decreasing the level of Aβ in the brain; reducing neuropathology associated with Alzheimer's disease; reducing inflammation and/or oxidant stress in the brain; improving memory and/or learning; treating other conditions involving Aβ/RAGE interaction at the blood-brain barrier, RAGE-mediated transport of Aβ into the brain, or RAGE activation in brain vasculature and/or brain parenchyma (e.g., diabetic complications); or any combination thereof.
EP2425830A1 Synergistic drug combination for the treatment of cancer The present invention relates to synergistic drug combinations and the use of said drug combinations for the treatment of proliferative diseases.
CN1637010A Extraction and application of paeonol amygdaloside The present invention discloses the extraction and application of paeonol amygdaloside as one kind of organic compound. The compound may be used in preparing medicine for preventing and treating hypertension, hemicrania and other reacting source diseases.
CN101057847A Polyhydroxy piperidines compound and preparation method and application thereof The invention discloses the use of polyhydroxy piperidine compounds having a general formula (I) in preparing hypoglycemic medicaments.
CN103102382A Crystal form B of glycyrrhetinic acid-30-amide derivative and preparation method thereof The invention provides a crystal form compound of N-[(3-o-chlorophenyl-isoxazol-5-yl)methyl]-11-desoxy-glycyrrhetinamide, namely a crystal form B. The invention also provides a method for preparing the crystal form B. The invention also provides a pharmaceutical composition containing the crystal form used as an active ingredient. The invention simultaneously provides application of the crystal form in the preparation of adrenal cortical hormone replacement medicaments, such as anti-inflammation, anti-allergy and the like. The crystal form can be also used for the preparation of liver protection medicaments, antiviral medicaments and the like.
CN101757621B Cyclodextrin inclusion drug composition for ocular inflammation resistance The invention relates to a cyclodextrin inclusion drug composition for ocular inflammation resistance, which consists of vitamin C or a derivative thereof as an active ingredient, glucocorticoid, cyclodextrin and one or more pharmaceutically acceptable pharmaceutical excipients capable of acting on eyes, wherein the glucocorticoid and/or the derivative of the vitamin C are included by the cyclodextrin.
US7268146 (3,4-Dihydro-1H-isoquinolin-2-yl)-[2-methyl-7-(2,4,6-trimethyl-phenyl)-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-b]pyridin-3-yl]-methanone; Corticotropin releasing factor (CRF); stress-related illnesses, mood disorders such as depression, major depressive disorder, single episode depression This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein Ar is optionally substituted aryl or heteroaryl, R1-R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.
US20120269904 Solution containing hypochlorous acid and methods of using same The present invention relates to low pH antimicrobial solutions comprising hypochlorous acid, water, and, optionally, a buffer. The inventive low pH antimicrobial solutions have a pH from about 4 to about 6 and are useful for treating impaired or damaged tissue and for disinfecting surfaces. Chemical processes for the production of the low pH antimicrobial solutions are also provided wherein chlorine gas is added to a buffer solution containing a buffering agent and water. The present invention also provides an electrochemical process for the production of the low pH antimicrobial solutions.
CN1843403A Red salvia root and ligustrazine transfusion liquid and its preparation process The invention relates to a transfusion for treating obliteration cerebrovascular diseases and its preparing process, wherein the transfusion is prepared from radix salvia miltiorrhiza 50-400g, hydrochloric ligustrazine 5-40g, osmoregulation agent 450-50000g, stabilizing agent 0-150000g, water for injection 50-500L. The medicament can be used for intra-vascular instillation.
CN1583758A Use of Maituolaicin Maituolaimeisu is used to prepare a medicine against virus, eg, Coxsackie B6 or viruses caused human Immunodeficiency. It is verified by experiment that it has inhibition to coxsackie B6, better than virus azoles in current clinic with safe indexs higher. It shows activeness against viruses caused human Iimmunodeficiency virus Ppoteinase.
CN101600431A Pharmaceutical composition having improved storage stability Disclosed is a pharmaceutical composition containing a compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof, while having improved storage stability. Specifically disclosed is a pharmaceutical composition containing (A) a compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof, and (B) a water-soluble polymer.
WO2007009709A1 Cycloalkane-substituted pyrazoline compounds, their preparation and use as medicaments The present invention relates to Cycloalkane-substituted substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
CN1943591B Castrating liquid for animal An animal castrating solution is presented and said solution mainly consists of phenol, common salt and phenyl methanol and characterized by including calcium chloride , and its formula of percentage by weight is as follows: phenol 4-7 , common salt 10-17, phenyl methanol 3-5, calcium chloride 3-5, the remainder being water. Using one kind of said animal castrating solution in said invention canreplace the original two kinds, both male and female animals can be castrated by means of injection and pouring into, meanwhile the merits of the original one are maintained.
CN101732330B Phtneolamine mesilate and fructose composition, preparation method thereof and use thereof The invention provides a phtneolamine mesilate and fructose composition, in which the concentration of the phtneolamine mesilate is 0.005 to 0.05 percent (w/v), the concentration of fructose is 5 to 10 percent (w/v), and the pH value is 5.0+/-0.1. The invention also provides a preparation method of the phtneolamine mesilate and fructose composition. The prepared composition can be taken by parturient with pregnancy induced hypertension and diabetes for quickly, safely and smoothly control blood pressure, has the advantages of high treatment effect, small side effect, convenient storage and the like and has simple preparation process and is convenient to promote.
EP1986994A2 Novel crystalline forms of armodafinil and preparation thereof The invention encompasses crystalline forms of armodafinil , processes for preparing the crystalline forms, and pharmaceutical formulation.
CN1969860A Method for preparing colon targeted pill of ofloxacin used for poultry and livestock The invention discloses a floxacin Hydrochloride colon targeting pill of flock, which comprises the following parts: fluorobenzenenicore as drug layer, 8% ethol as retarding layer, 2% HPMC as time lag layer and 15% S100 as sensitive film.
CN103251612A Application of Aspeverin in preparation of medicines for treating rheumatoid arthritis The invention discloses Aspeverin for treating immune inflammation. The Aspeverin is used for preparing medicines for treating rheumatoid arthritis and has an exact curative effect by using terfenadine and diclofenac sodium as control. An application of Aspeverin in preparation of medicines for treating rheumatoid arthritis is disclosed for the first time, a framework type belongs to a brand-new framework type, the Aspeverin has an unexpected strong effect of inhibiting the rheumatoid arthritis activity, and the revelation possibility of other compounds cannot be generated, so the application has obvious substantive features; and moreover, the application has an obvious improved effect of preventing the rheumatoid arthritis.
CN101307047A Heterocyclic compounds and applications thereof as antineoplastic drugs The invention discloses a heterocyclic compound, pharmaceutically acceptable salt thereof and a method for preparing the heterocyclic compound. The heterocyclic compound can be used for tumor therapy.
EP1676918A2 G-beta-gamma regulated phosphatidylinositol-3' kinase The present invention relates to the discovery, identification and characterization of nucleotides that encode the G protein regulated phosphatidylinositol-3' kinase, a heterodimeric enzyme which produces the intracellular messenger phosphatidylinositol (3, 4,5)-triphosphate in response to activation of trimeric G protein-linked receptors. This novel protein, comprised of a catalytic subunit, p120, and a regulatory subunit, p101, is found in cells of hematopoietic origin and is involved in immune system responses which cause inflammation. The presence of p101 subunit is largely responsible of the dramatic stimulation of kinase activity in the presence of activated trimeric G proteins. The invention encompasses p101 and p120 nucleotides, host cells expression systems, p101 and p120 proteins, fusion proteins, polypeptides and peptides, antibodies to these proteins, transgenic animals that express a p101 or p120 transgene, or recombinant knock-out cells and animals that do not express the p101 or p120 genes, antagonists and agonists of the enzyme, and other compounds that modulate p101 or p120 gene expression or enzyme activity that can be used for diagnosis, drug screening , clinical trial monitoring, and/or treatment of inflammatory disorders.
WO2013173428A1 Veliparib in combination with whole brain radiation therapy for the treatment of brain metastases The invention relates to a method for the treatment of brain metastases from non-small cell lung cancer in a subject, comprising administering to the subject an effective amount of 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of whole brain radiation.
WO2011097456A2 Compositions and methods for enhanced parvovirus transduction The present invention provides methods and compositions for enhanced transduction of an adeno-associated virus (AAV) vector comprising a heterologous nucleic acid of interest wherein the AAV vector genome is oversized relative to a wild type AAV genome by employing a proteasome inhibitor.
WO2012132913A1 Clostridium difficile growth inhibitor Provided are: a Clostridium difficile growth inhibitor which comprises, as the active ingredient, a propionic acid bacterium and/or a fermentation product thereof; and a prebiotics composition which has an effect of inhibiting the growth of Clostridium difficile. Also provided are: a Clostridium difficile growth inhibitor which comprises, as the active ingredient, 1,4-dihydroxy-2-naphthoic acid (DHNA) and/or an organic acid; a prebiotics composition which has an effect of inhibiting the growth of Clostridium difficile; and a food composition comprising the same. Also provided is a method for inhibiting the growth of Clostridium difficile, said method comprising taking or administering the aforesaid substances.
CN101829085A Application of ring A dioxane flavonolignan in preparing medicaments for resisting hepatitis B viruses (HBV) The invention relates to application of ring A dioxane flavonolignan in preparing medicaments for resisting hepatitis B viruses (HBV), in particular to application of ring A dioxane coupling type flavone lignan or a pharmaceutically acceptable salt thereof in preparing medicaments for clearing away hepatitis B e antigen (HBeAg), suppressing the HBV DNA replication and treating HBV infection diseases. The flavonolignan has certain activity on resisting the HBeAg, and the intensity of the flavonolignan for clearing away the HBeAg is higher than that of Lamivudine which is a positive control and close to that of 10,000 units/milliliter of alpha-interferon. Meanwhile, the suppression ratio of the compound to the HBV DNA replication is higher than 80 percent in the presence of a concentration of 100 micrograms/milliliter. The pharmacodynamical results indicate that the flavonolignan or the pharmaceutically acceptable salt thereof can be expected to be used for preparing the medicaments for clearing away the HBeAg, suppressing the HBV DNA replication and treating the HBV infection diseases.
CN102199171A Vanadium coordination compounds taking kojic acid derivative as ligand and preparation method and application thereof The invention provides vanadium coordination compounds taking a kojic acid derivative as a ligand and a preparation method and application thereof. The invention provides compounds show as a general formula (B). The preparation method for the compounds comprises the following steps of: preparing an organic micromolecular ligand from an antioxidant and kojic acid; and preparing new organic vanadium compounds from the organic micromolecualr ligand and vanadium-oxygen ions. The compounds solve the problem that vanadium compounds easily generate free radicals to cause oxidative stress so as to bring toxicity; and the organic micromolecular ligand is prepared from the kojic acid and the antioxidant and the new organic vanadium compounds are prepared from the ligand and the vanadium-oxygen ions. Animal experiments prove that: the vanadium coordination compounds taking the kojic acid derivative as the ligand have obvious effect of reducing blood sugar, and have low toxicity. The compounds have the general formula (B), wherein R refers to H, OH or OMe.
EP1753763A2 Indazole and indolone derivatives and their use as pharmaceuticals The present invention provides for compounds of formula (I), which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.
CN101601657A Amoxicillin soluble powder and preparation method thereof The invention relates to an amoxicillin soluble powder and a preparation method thereof, in particular to an amoxicillin soluble powder with anhydrous sodium carbonate as cosolvent and a preparation method thereof. The amoxicillin soluble powder comprises amoxicillin and anhydrous sodium carbonate with the weight ratio of 5-10:1. The preparation method of the amoxicillin soluble powder in the invention comprises the following steps: (1) crashing; (2) mixing the crashed amoxicillin powder and anhydrous sodium carbonate with the weight ratio of 5-10:1 evenly; and (3) split charging. The invention solves the problem of difficult dissolving of amoxicillin and overcomes the defect of bad amoxicillin effect in the existing technology.
US20070117180 Enzyme producing plasma protein fragment having inhibitory activity to metastasis and growth of cancer and plasma protein fragment produced by fragmentation by said enzyme An aspartic enzyme having a high homology with a cathepsin D precursor, which is a protein having the N-terminal amino acid sequence LVRIPLHKFT (SEQ ID NO: 1) and showing a molecular weight of about 45 kDa in non-reductive SDS electrophoresis and can degrade plasma proteins, typically plasminogen, to produce plasma protein fragments having an inhibitory activity to metastasis and growth of cancer; the plasma protein fragments having an inhibitory activity to metastasis and growth of cancer which is prepared via the degradation with the above enzyme; a process for preparing the protein fragments which comprises degrading plasma proteins with the above enzyme; and a medicament for treating and preventing metastasis and growth of cancer which comprises as a major ingredient the above enzyme or the plasma protein fragments.
US20080234292 Such as S)-(1-(1-Aminobicyclo[2.2.2]oct-4-yl)aminoacetyl)-2-cyanopyrrolidine; inhibitors of the enzyme dipeptidyl peptidase; antidiabetic agents The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR3 or O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.
WO2011027829A1 Composition containing rna derived from lactic acid bacterium as active ingredient Disclosed is a composition having an immunomodulatory activity, which contains RNA derived from a lactic acid bacterium as an active ingredient. Also disclosed is composition having a cytokine production control activity, which contains RNA derived from a lactic acid bacterium as an active ingredient.
CN103204894A Novel corosolic acid derivative, preparation method thereof and application thereof in preparing diabetes medicaments The invention relates to the technical field of natural medicinal chemistry and medicine, and discloses structures of two novel compounds 1 and 2 which have a general chemical structure as shown in a formula (1) and are obtained through converting corosolic acid by Cochliobolus lunatus, an extraction and separation method thereof, and an inhibition effect thereof on activity of alpha-glucosidase.
WO2012014221A1 Substituted 4-(4-fluoro-3-(piperazine-1- carbonyl)benzyl)phthalazin-1(2h)-one derivatives as poly (adp-ribose) polymerase- 1 inhibitors Disclosed are compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts. These compounds are suitable as Poly (ADP-ribose) polymerase- 1 inhibitors (PARP-1 inhibitors).
CN101384600A Crystalline forms of (3r,4r)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methol]piperidin-3-ol Crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol of the formula (I) are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases.
CN100999527A Selenaza aromatic heterocyclic compound with anti-tumor activty and its preparation process and application The present invention discloses one kind of selenic aromatic azacycle compound possessing antitumor activity in the structure as shown. The preparation process of the selenic aromatic azacycle compound includes the following steps: mixing diamine compound and selenium dioxide in the weight ration of 1 to 1 at room temperature and grinding; dissolving the product in cyclohexane and filtering; water washing and evaporating to eliminate cyclohexane and obtain pure product. The selenic aromatic azacycle compound possessing antitumor activity may be used in preparing antitumor medicine.
US20080146642 Propanesulfonic acid amino acid prodrugs that can deliver 3-amino-1-propanesulfonic acid (3APS) by minimizing metabolism associated with that drug, particularly compounds that block or protect amino group of 3APS such that it avoids metabolism by transaminases or monoamine oxidase; Alzheimer's disease The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to, the prevention and treatment of Alzheimer's disease.
WO2012153635A1 Therapeutic muscular dystrophy drug having bubble liposome loaded with morpholino as active ingredient The present invention addresses the problem of providing a technique for introducing a PMO of markedly improved cell permeability and of considerably improved introduction efficiency. The present invention thereby addresses the problem of providing a therapeutic drug for dramatically mitigating the pathological condition of DMD. The present invention provides a therapeutic drug for Duchenne muscular dystrophy, the drug being characterized in containing as an active ingredient a bubble liposome having a specific morpholino oligomer (PMO) bound to the surface, and characterized in that ultrasonically irradiating muscle tissue from outside the body after administration to muscle tissue or a blood vessel causes the PMO to be introduced with high efficiency into the muscle fiber (muscle cells) of the muscle tissue.
CN102153529B Single-tetrahydrofuran-type annonaceous acetogenin compounds with antitumor activity and application thereof The invention discloses new single-tetrahydrofuran-type annonaceous acetogenin compounds with antitumor activity. In the invention, based on systemic deep research on the chemical composition of anonaceae seed, wave spectrometric and mass spectrometric data analysis shows that two new single-tetrahydrofuran-type annonaceous acetogenin compounds (Annonacins I and II) are separated from anonaceae seed; in-vivo and in-vitro antitumor activity researches show that the single-tetrahydrofuran-type annonaceous acetogenin compounds provided by the invention have strong antitumor activity on various tumor cells including lung cancer, breast cancer, liver cancer, cervical carcinoma and gastric cancer; toxicity test researches show that the single-tetrahydrofuran-type annonaceous acetogenin compounds with antitumor activity, provided by the invention, have low toxicity and are expected to be developed into new antitumor drugs.
CA2386685C Use of pleuromutilin derivatives for transdermal treatment of bacterial diseases Described is the use of a compound of formula (I) wherein the substituents have the meanings given in claim 1, for the manufacture of a medicament for the transdermal treatment of bacterial infections m humans and animals. Further described are transdermal compositions for said treatment.
US20110023135 Use of a new gene coding for a new member of the mcm2-8 family in pharmaceutical compositions The use of the human or animal MCM9 gene, or parts of the gene, or transcripts thereof, or antisense nucleic acids able to hybridize with part of the gene or transcripts, or silencing RNA derived from parts of the transcripts and able to repress the MCM9 gene, or proteins or peptidic fragments translated from the transcripts, or antibodies directed against the proteins or peptidic fragments, for the preparation of a pharmaceutical composition for the treatment of a human or animal pathology linked to a dysfunction of the expression of the MCM9 gene, or of human or animal cancers.
CN101966148A Injection composition comprising coenzyme Q10 and preparation method thereof The invention discloses an injection composition comprising a coenzyme Q10. The invention is characterized in that: the injection composition taking an oxidized coenzyme Q10 as a main functional raw material also comprises an emulsifier, aids, a surfactant and a solvent, wherein the adopted emulsifier is polyethylene glycol or glycerol, or a mixture of the polyethylene glycol and the glycerol; the aids are various vitamins and amino acids needed by a human body or a mixture of the vitamins and amino acids; the surfactant is Tween-20 or hydroxypropyl methyl cellulose; and the solvent is physiological saline or deionized water. Meanwhile, the injection composition is prepared from the following components in percentage by weight: 3.0 to 30 percent of reduced coenzyme Q10, 0 to 20 percent of emulsifier, 0 to 15 percent of aids, 0 to 10 percent of surfactant and the balance of solvent.
US20080021012 3-[4-{6-Substituted Alkanoyl Pyridin-3-Yl}-3-Phenyl]-5-(1H-1,2,3-Triazol-1-Ylmethyl)-1,3-Oxazolidin-2-Ones As Antibacterial Agents Compounds of formula (I) as well as pharmaceutically-acceptable salts and pro-drugs thereof are disclosed wherein R1, R2, R3, and R4 are defined herein. Also disclosed are processes for making compounds of formula (I) as well as methods of using compounds of formula (I) for treating bacterial infections.
US20090197930 Eyedrops It is intended to provide eyedrops which have an ocular tension-lowering effect and a hypotensive effect based on novel function mechanisms. The above-described eyedrops contain a muscle relaxant as the active ingredient and dantrolene sodium is preferably usable as the muscle relaxant employed as the active ingredient. The eyedrops lower the ocular tension via the relaxation of the extraocular muscle tension and lower the blood pressure via the relaxation of the sympathetic nerve tension, thereby exhibiting the ocular tension-lowering effect and the hypotensive effect.
WO2007056513A1 α-HELIX MIMETICS AND METHODS RELATING TO THE TREATMENT OF FIBROTIC DISORDERS The invention provides α-mimetic structure of formula (I), wherein A is -(C=O)-CHR3-, or -(C=O), B is N-R5- or -CHR6-, D is -(C=O)-(CHR7)- or - (C=O)-, E is -(ZR8)- or (C=O), G is -(XR9)n-, -(CHR10)-(NR6)-,-(C=O)-(XR12)-, -(C=N-W-R1)-, -(C=O)-, X-(C=O)-R13,X-(C=O)-NR13R14,X-(SO2)-R13, or X-(C=O)-OR13, W is -Y(C=O)-, -(C=O)NH-, -(SO2)-, -CHR14, (C=O)-(NR15)-, substituted or unsubstituted oxadiazole, substituted or unsubstituted triazole, substituted or unsubstituted thiadiazole, substituted or unsubstituted 4,5 dihydrooxazole, substituted or unsubstituted 4,5 dihydrothiazole, substituted or unsubstituted 4,5 dihydroimidazole, or nothing, Y is oxygen or sulfur, X and Z is independently nitrogen or CH, n=0 or 1 ; and R1, R2, R3, R4, R5, R6, R7, R8, R9 R10, R11, R12, R13, R14, and R15 are the same or different and independently selected from an amino acid side chain moiety or derivative thereof, the remainder of the molecule, a linker and a solid support, and stereoisomers, salts, and prodrugs thereof, provided that where B is CHR6 and W is -Y(C=O)-, -(C=O)NH-, -(SO2)-, -CHR14, or (C=O) (NR15)-, G cannot be CHR9, NR9, (C=O)-CHR12, (C=O)-NR12, or no atom at all. Additionally, the invention provides methods wherein α-mimetic compounds are used to treat fibrotic disorders.
US20070155808 G Protein-Coupled Receptors (GPR40); insulin secretagogue; diabetes; 3-[4-[[4-[[(2-Phenylethyl)(4-phenyl-1,3-thiazol-2-yl)amino]methyl]benzyl]oxy]phenyl]propanoic acid The present invention provides a novel compound having a GPR40 receptor function modulating action, which is useful as an insulin secretagogue, a drug for the prophylaxis or treatment of diabetes and the like. A compound represented by the formula (I) wherein each symbol is as defined in the specification, a salt thereof and a prodrug thereof have unexpectedly superior GPR40 receptor agonist activity and also show superior properties as a pharmaceutical product, such as stability and the like. Thus, they can be safe and useful drugs for the prophylaxis or treatment of GPR40 receptor related conditions or diseases in mammals.
CN103272223A Oxidation prevention health care capsule and preparation method thereof The invention provides an oxidation prevention health care capsule and a preparation method thereof. Taking 300g capsule as total weight, the capsule is manufactured by the following components: 20-30 g 80% wt of ginsenoside power, 0.8-1.5 g ox blood extraction SOD, 15-25 g vitamin C, and 25-35 g vitamin E powder and filler of margin. Compared with the conventional anti-oxidant health care capsule, the capsule provided by the invention comprises the ginsenoside, the ox blood extraction SOD, the vitamin C, and the vitamin E, wherein the ox blood extraction SOD belongs to an enzyme anti-oxidant; the vitamin E and the vitamin C belong to non-enzyme anti-oxidants; and two anti-oxidants combine with the ginsenoside with the effect of adjusting the overall function of an organism to play the effect of oxidation prevention together. The oxidation prevention capsule provided by the invention makes full use of free radical eliminating mechanism of each tissue and organ, comprises materials with different oxidation prevention mechanisms, and improves the efficiency of oxidation prevention.
US20100137411 Ras-mediated epigenetic silencing effectors and uses thereof The invention relates to methods for inhibiting gene silencing, methods for inhibiting cell proliferation, methods for inhibiting Ras mediated tumor growth, methods for screening for regulators of FAS expression, and methods for identifying inhibitors of Ras mediated tumor growth.
WO2009005459A1 Phenyl-1,2, 3,4-tetrahydroisoquinolinone derivatives and their use in the treatment of a pain disorder The present invention relates to new compounds and pharmaceutically-acceptable salts thereof, and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
US7345172 Intercalation compound for use in the diagnosis and detection of genetic disorders; sterically demanding nucleotide intercalating compounds and methods for detecting base pair mismatches in nucleic acid sequences In accordance with the present invention there is provided a new class of sterically demanding metallo-intercalators. These compounds intercalate between bases in a duplex polynucleotide, but only where the bases are not fully complementary, for example, where there is a base-pair mismatch. The compounds are sufficiently sterically demanding that intercalation between bases in fully complementary duplexes does not occur to a significant degree. These mismatch intercalators are useful for detecting DNA and RNA defects, for diagnosing disorders characterized by the presence or increase in DNA and/or RNA defects, and for treating such disorders. Further, the compounds are capable of catalyzing photolytic cleavage of nucleic acids at relatively long wavelengths, and under normal sunlight.
CN101653413B Tacrolimus ophthalmic emulsion and its preparation method The invention provides a tacrolimus ophthalmic emulsion and its preparation method, which belongs to the medicine preparation technical field and solve the problems of high toxic and side effects of tacrolimus oral preparation and injection to human body in the prior art. The emulsion is composed of tacrolimus, oil phase, an emulsifier, an auxiliary emulsifier, an osmotic pressure modifying agent, an antioxidant, a preservative, a pH modifying agent and an injection water, is prepared by an ultrasonic shearing emulsification or shearing-high pressure homogenization technology and is applied to treatment of ophthalmic corneal allograft rejection, keratoconjunctivitis sicca (KC) and ophthalmic anaphylactic disease. The invention prepares the tacrolimus into the ophthalmic emulsion for the first time, has the advantages of good biological compatibility, low stimulation to eyes and no toxic and side effects in the long-term application and can be applied clinically with wide development prospects.
US20060122264 Stem cell invasion inhibitor The present invention provides an inhibitor of the invasion of bone-marrow-derived vascular stem cells or inflammatory cells into blood vessel walls, a blood vessel restenosis inhibitor, and a preventive or therapeutic drug for angiitis or myocardiitis, each containing a phthalein dye compound as an active ingredient; and an instrument for treating blood vessels which is coated with a resin containing a phthalein dye compound or made of such a resin. Use of the drug of the present invention enables effective prevention of restenosis of a blood vessel after, for example, angioplasy. Moreover, it is possible to prevent the progress and disruption of a lesion of angiitis, myocarditis, or arterioscrelosis, for which no efficacious preventive or therapeutic method has been established so far, as well as microvascular ischemic diseases. By performing a medical treatment such as angioplasy using the instrument of the present invention for treating blood vessels, events of vascular restenosis can be effectively prevented.
WO2006081337A2 Erastin analogues and their uses for killing cancer cells The invention provides methods for effective killing of cancer cells with erastin and related compounds or derivatives.
CN102863512A Novel antiviral compound The invention relates to a compound with a structure represented by a general formula I, or an enantiomer, a diastereomer, a resonator, or a pharmaceutically acceptable salt or a solvate of the compound, wherein the symbols are defined in the specification; and the compounds with the similar pharmaceutic components are utilized to treat or prevent virus infection, such as virus similar to HIV (human immunodeficiency virus).
US20050245463 Novel antiretroviral sulfolipids extracted from spirulinae, method for obtaining same, compositions containing same and use thereof as inhibitors of the hiv virus reverse transcriptase The invention relates to novel sulfolipids extracted from spirulins, to the process for obtaining them, to the compositions containing them and to their use as HIV-1 and HIV-2 inhibitors. The invention further relates to a spirulin biomass rich in sulfolipids which has an inhibitory activity towards HIV-1 and HIV-2 reverse transcriptase, and to the use of said sulfolipids, or of an extract of spirulin biomass rich in sulfolipids, for the preparation of a drug for the prophylactic or curative treatment of AIDS.
US20070010517 Pharmaceutical salts of reboxetine The present invention relates to novel crystalline, water-soluble salts of the 2S,3S enantiomer of reboxetine, which are the fumarate and succinate salts thereof, to a process for their preparation, to their utility in therapy and to pharmaceutical corn-positions containing them.
US20060211689 Aminoquinoline derivatives and their use as adenosine A3 ligands The present invention relates to an adenosine A3 receptor ligand of the general formula (I), within those preferably to the antagonists, including a salt, solvate or isomer (tautomer, desmotrop, and optically active isomer) thereof, to a pharmaceutical composition containing the ligand, to the use of the ligand, to its preparation, and intermediates of the ligand of the general formula (II″), (III″), (IV″), (V″), (VI″), (VII″), (VIII″) and (XIII″) and their preparation.
CN1951483B Hybrid safflower oil and preparation method thereof The invention discloses a safflower oil and process for preparation, wherein the main constituents include methyl salicylate, eucalyptus oil, citronella oil, clove oil, thymol, tea seed oil. The preparing process consists of steps of mixing homogeneously, charging tea seed oil and filtering. The obtained product contains C8H8O3 50.0-61.2% (g/g).
CN103102271A Industrialized preparation method of guacetisal and medical application of dry suspension The invention discloses an industrialized preparation method of guacetisal, which comprises the following steps: based on salicylic acid and guaiacol as raw materials, carrying out esterification on the raw materials so as to obtain salicylic acid-guaiacol ester; and then, carrying out acetylization on hydroxy so as to obtain guacetisal, wherein in the esterification reaction, one of pyridine, 4-dimethylamino-pyridine and dimethylformamide is selected as a catalyst; and in the step of carrying out acetylization on hydroxy, one of pyridine, 4-dimethylamino-pyridine and dimethylformamide is added and used as an auxiliary alkali reagent. According to the invention, the technological production cost is low, the synthetic route is short, the reaction rate is improved, and the reaction temperature is reduced, so that the reaction temperature is milder and the preparation method is suitable for industrialized production; the post-treatment processes of esterification and acetylization reactions are simple, complicated quenching, extraction and solvent replacement operations are avoided, the time of batch production is greatly reduced, and the application amount of organic solvents is maximally reduced; and therefore, the industrialized preparation method of guacetisal is particularly suitable for industrialized production.
CN1868454A Slow-release injection contg. platinum compounds and its potentiator A slow-release anticancer injection is composed of the slow-release micro-balls containing active component and slow-releasing auxiliary and the special solvent containing the suspending aid. Said active component is the combination of Pt compound chosen from dicycloplatinum, etc and the topological enzyme inhibitor and/or tetraazine compound. Said slow-releasing auxiliary is chosen from polylactic acid or its copolymer, monoethyl polyethanediol or its copolymer, EVAc, etc.
US20120046263 Method to alter sex ratios in avian offspring The present invention includes methods of influencing the sex chromosome ovulated by a female bird and altering the sex ratio in avian offspring by altering the exposure of an ovulating female bird to one or more stress hormones. In some aspects, the method includes exposing an avian female to a glucocorticoid, such as for example, corticosterone, after the completion of rapid yolk deposition and prior to ovulation
CN101773478B Pulmonary targeting microsphere of veterinary ceftiofur hydrochloride and preparation method thereof The invention provides a pulmonary targeting microsphere of veterinary ceftiofur hydrochloride and a preparation method thereof, which solves the problems of the prior art that the quantity of microspheres reaching the target site is small, thereby causing a large amount of drug waste, the therapeutic effect is no significant, the side effects of drugs are increased, and the possibility for generating drug resistance is high. In the technical scheme of the pulmonary targeting microsphere of veterinary ceftiofur hydrochloride, ceftiofur hydrochloride is used as a main component, poly-lactic-co-glycolic acid is used as a carrier material, and the mass ratio of the ceftiofur hydrochloride and the poly-lactic-co-glycolic acid is 1:1-1:50. The preparation method adopts the spray drying method.The particle sizes of the microspheres prepared in the method are relatively uniform, the large-scale preparation can be realized, the drug loading capacity and the encapsulation efficiency are both high, more than 89 percent of the particle sizes of the microspheres are all between 7mum and 30mum, thereby meeting the requirements of the pulmonary targeting microspheres for the particle sizes, and the microspheres can be concentrated in the lung, thereby enhancing the therapeutic effect.
WO2007023774A1 Agent for amelioration of impaired ophthalmic arterial blood flow Disclosed is an agent for amelioration of impaired ophthalmic arterial blood flow. Also disclosed is a method for amelioration of impaired ophthalmic arterial blood flow. An agent for amelioration of impaired ophthalmic arterial blood flow comprising an anthocyanin as an active ingredient; and an agent for treatment or prevention of a disease or disorder associated with impaired ophthalmic arterial blood flow.
WO2007044547A1 Methods for achieving and maintaining weight loss Methods for achieving weight loss goals and maintaining weight loss including selecting an appropriate weight loss program and identifying a weight loss goal, followed by participating in the weight loss program until the weight loss goal is achieved; then ending the weight loss program participation; and consuming an ingestible composition at regular intervals beginning from 1 day to about 7 days after ending the weight loss program, the ingestible composition comprising an effective amount of a multivalent cation and an effective amount of an soluble anionic fiber.
CN1923791A Preparation method of Suillin and application thereof The invention discloses a preparing method of Suillin with molecular formula as C28H40O4 and molecular weight at 440 and application in the antitumor agent, which is characterized by the following: grinding vacuum freeze dried Suillin into dried powder; adding acetic ester to extract under indoor temperature; filtering; evaporating filtrate; condensing; recycling the concrete on the back-phase silica gel column; proceeding gradient elution; collecting biological eluted material; condensing; dissolving C8 back-phase through solvent to prepare column; separating; purifying.
EP2213308A1 Eyedrop comprising agar It is intended to prepare a composition which contains polysaccharide at a high concentration and yet remains in the state of a liquid having low viscosity to thereby provide drugs, eyedrops, foods, cosmetics, toiletry products having a novel texture or function. The composition in the state of a liquid having low viscosity is obtained by heating polysaccharide at a high concentration in a water-containing liquid and then cooling under applying a shear force, which enables the provision of the above-described drugs. The composition is usable as an aqueous drug vehicle which is free from gelling due to temperature changes during storage and easily applied without pouring and/or streaming down. Eyedrops containing agar have an effect of enhancing ocular drug penetration. Eyedrops containing particulate agar maintain a low viscosity and, achieve easy instillation and impart a favorable feel in instillation.
EP2487159A1 RorgammaT inhibitors The present invention relates to compounds according to general Formula I or a pharmaceutically acceptable salt thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
US7569574 Purine derivatives, the preparation thereof and their use as pharmaceutical compositions The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV), the preparation thereof, the use thereof for the prevention or treatment of diseases or conditions associated with an increased DPP-IV activity or capable of being prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, the pharmaceutical compositions containing a compound of general formula (I) or a physiologically acceptable salt thereof as well as processes for the preparation thereof.
US20110124638 Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors There is provided a compound of formula I: , or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
WO2006109898A1 Antimicrobial composition containing natural extract, nano silver and natural essential oil The present invention relates to a composition containing grapefruit, purslane (Portulaca oleracea L.) and Houttuyniae Herba {Houttuynia cordata Thunb) extracts as natural extracts, nano silver and natural essential oils, and having excellent antimicrobial activity. The antimicrobial composition in accordance with the present invention comprises 10 to 30% by weight of natural extracts containing a 1 : 1 : 1 mixture (w/w) of grapefruit, purslane {Portulaca oleracea L.) and Houttuyniae Herba {Houttuynia cordata Thunb) extract, 1 to 5% by weight of nano silver having a concentration of 50 to 1,000 ppm, 5 to 30% by weight of a mixture of natural essential oils and the balance of ethanol. The antimicrobial composition in accordance with the present invention exhibits excellent antimicrobial activity against bacteria and fungi such as Staphylococcus aureus, resident skin flora and Dermatophytes, and is suitable for preparation of formulations comprising the antimicrobial composition and having antimicrobial activity, such as hand cleaning agents, aromatic fragrances and herbal gels.
US20060178417 4-[6(2,2-dimethylpropanoyloxy)indan-1-ylmethyl]1H-imidazole, an alpha 2 adrenergic agonist, for the treatment of hypertension, glaucoma, headaches, diarrhea, ischemia, drug abuse and dependence, hypotension, shock, congestive heart failure, anxiety, as decongestants, analgesics or as sedatives Novel prodrugs of MPV-2426, methods for preparing said prodrug forms, pharmaceutical compositions containing such prodrug forms, and methods for using the prodrug forms. A compound of general formula (I), or pharmaceutically acceptable salts or hydrates thereof, wherein R represents unsubstituted or substituted lower alkyl, unsubstituted or substituted aryl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted heteroaryl, unsubstituted or substituted lower alkylamino or a saturated five or six membered heterocyclic group containing one or two nitrogen atoms.
CN103599174A Composition for improving bone mineral density The invention discloses a composition for improving the bone mineral density. The composition is prepared by adopting L-asparaginic acid chelated calcium and pueraria isoflavones as main raw materials. The composition is especially suitable for postmenopausal women to eat.
US20080269216 Gastrointestinal disorders; irritable bowel syndrome The present invention relates to novel compounds having a positive allosteric GÀBAB receptor (GDR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). A compound of the general formula I
US20120258162 Controlled delivery of molecules from a biointerface Disclosed are methods and apparatuses for delivery of bioactive molecules. The drug delivery systems include an implantable medical device which significantly reduces or suppresses adverse biological responses associated with implantable devices and also promotes vascularization in tissues surrounding the implanted device. The disclosure also relates to drug delivery systems designed to vary the rate of delivery of bioactive molecules with a change in the physiological environment.
US20120046261 Compositions and methods for diagnosing and preventing spontaneous preterm birth Disclosed herein are compositions and methods of identifying a subject at risk for preterm birth and selecting effective therapies for preventing preterm birth in the subject. The disclosed methods generally involve determining the identity of one or more nucleotides in the progesterone receptor (PR) gene of the subject.
US20100247627 Foxn1 and pigmentation The present invention provides methods and compositions for modulating skin pigmentation.
CN101822689A Medicament compound containing hyaluronic acid and beta-aescine sodium The invention provides a medicament compound containing hyaluronic acid and beta-aescine sodium and application thereof in preparing medicaments for treating diseases of osteoarthritis and the like. The compound can play the function of the hyaluronic acid for treating osteoarthritis and the function of the beta-aescine sodium for resisting inflammation and free radicals. In addition, used as an inhibitor of hyaluronidase, the beta-aescine sodium can delay the degradation of the hyaluronic acid by the hyaluronidase, thereby the curative effect is remarkably delayed and improved, and the occurrence of complications is reduced.
US7417072 Blockade of Pin1 prevents cytokine production by activated immune cells The invention provides pharmaceutical compositions and methods of treating immunological disorders. The invention also provides pharmaceutical compositions and methods of inducing eosinophil apoptosis, and methods for treating eosinophil-associated disorders comprising inducing eosinophil apoptosis in an individual in need thereof.
EP2350664A1 Treatment of cancer using hypoxia activated prodrugs Cancer can be treated by administration of a hypoxia-activated prodrug, such as TH-302, alone or in combination with other anticancer agents and/or radiation therapy. In combination therapy, the hypoxia-activated prodrug and another anticancer agent or radiation therapy may be administered within the same 24-hour period, and administration of the hypoxia-activated prodrug may be completed prior to beginning administration of the other anticancer agent or radiation therapy.
US20080070898 Sodium channel inhibitor of low side effect; analgesics; neuropathic pain; 4-(2-{4-[(E)-2-(2-methylphenyl)vinyl]piperidin-1-yl}-2-oxoethyl)morpholine for example The piperidine derivative of the present invention in which the 4-position of the piperidine ring is bonded, via vinylene, to a mono-substituted (—R1) or unsubstituted benzene ring and the 1-position of the piperidine ring has an acyl group [—C(═O)—R4], or a pharmaceutically acceptable salt thereof has an excellent sodium channel inhibition action and an excellent analgesic action and shows a high analgesic effect particularly to neurogenic pain. The present compound is useful as a sodium channel inhibitor of low side effect
US20090075972 Use of Midostaurin for Treating Gastrointestinal Stromal Tumors The present invention relates to the use of midostaurin, in free form or in pharmaceutically acceptable salt form in the manufacture of a pharmaceutical composition for the treatment of gastrointestinal stromal tumors, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of midostaurin is administered to an animal suffering from said disease or condition.
CN101244054A Application of oridonin in preparing medicaments for promoting surrounding vascellum tunica interna incrassation The invention discloses an oridonin application in preparation of the medicine accelerating the thickening of the peripheral blood vessel intima; wherein, the peripheral blood vessel is relative to the solid tumor therapy, the medicine is the preparation of oridonin. The peripheral blood vessel intima is thickened by the oridonin provided by the invention injected by vein bolus injection, thus, the lumen is narrowed even obstructed and the blood supply of the solid tumor is stopped, at last the aim of tumor inhibitory is achieved.
EP2310381A1 2,4'-bipyridinyl compounds as protein kinase d inhibitors useful for the treatment of ia heart failure and cancer The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
US20100261691 Amorphous form of an anti-inflammatory compound The invention relates to the technical field of anti-inflammatory compounds, specifically those of a steroid nature, in particular to a new amorphous form of a nitrooxy derivative of a corticosteroid, its pharmaceutical formulations and its use in the treatment or prevention of diseases or symptoms of the skin or mucous membranes.
CN1810244A Freeze dried Lansoprazole sodium injection and its prepn process The freeze dried Lansoprazole sodium sdinjection has Lansoprazole sodium as active component and mannitol or meglumine as excipient in the weight ratio of 15-30 g to 5-50 g. The preparation process of the freeze dried Lansoprazole sodium injection includes the following steps: dissolving Lansoprazole sodium in 15-30 g in injection water of 200-400 ml, dissolving mannitol or meglumine as excipient in 5-50 g in injection water of 100-300 ml, mixing the two kinds of obtained solutions and adding injection water to 2000-3000 ml, adding active carbon in 0.5-1.5 g, filtering with microporous filter membrane, packing in vial, freeze drying under bacteria-free condition, and pressing cap. The freeze dried Lansoprazole sodium injection is used clinically in intravenous drip or intramuscular injection to treat peptic ulcer and other diseases.
US20050079167 Surface treated active carbon; controlling particle size, porosity An adsorbent for oral administration, characterized by comprising a spherical activated carbon prepared from a thermosetting resin as a carbon source, wherein a diameter is 0.01 to 1 mm, and a specific surface area determined by Langmuir's adsorption equation is 1000 m2/g or more; and an adsorbent for oral administration, characterized by comprising a surface-modified spherical activated carbon prepared from a thermosetting resin as a carbon source, wherein a diameter is 0.01 to 1 mm, a specific surface area determined by Langmuir's adsorption equation is 1000 m2/g or more, a total amount of acidic groups is 0.40 to 1.00 meq/g, and a total amount of basic groups is 0.40 to 1.10 meq/g. The adsorbents for oral administration exhibit a useful selective adsorbability, that is, a less adsorbability of useful substances in a body, and a greater adsorbability of toxic substances.
WO2006047891A1 Polycyclic aromatics and derivatives thereof and processes for their preparation This invention relates to novel biologically active polycyclic aromatics produced by cultivation of Micromonospora echinospora ssp. challisensis NRRL 12255. The invention also relates to their pharmaceutically acceptable salts, prodrugs and derivatives, and to methods of obtaining them by post-biosynthesis chemical modification. The invention further relates to the use of the polycyclic aromatics and their derivatives in the preparation of medicaments for the treatment of neoplastic conditions and bacterial infections.
CN102218068A Application of PPARgamma stimulant 15d-PGJ2 to preparation of targeting liver cancer stem cell drugs The invention discloses the application of a PPARgamma stimulant 15d-PGJ2 to the preparation of targeting liver cancer stem cell drugs. Through research, it is found that the PPARgamma stimulant 15d-PGJ2 has an effect on the CD133+ liver cancer stem cell subgroup. The result shows that the PPARgamma stimulant 15d-PGJ2 can effectively inhibit the growth of the CD133+ liver cancer stem cell subgroup, reduce the rate of the CD133+ subgroup in a liver cancer cell line, decrease the in vitro monoclonal formation and balling capabilities of liver cancer cells, and simultaneously reduce the expression of stem cell related genes of liver cancer cells. The research indicates that PPARgamma can be taken as the target for inhibiting liver cancer stem cells and provides the experimental basis for developing effective targeting liver cancer stem cell drugs.
US20080182860 Pyrimidine Compounds as Purine Receptor Antagonist Compounds of formula (1); wherein R1 is optionally substituted C1-C3alkyl C2-C3alkenyl, or C2-C3alkynyl, or —NR6R1, —ORB, —SR9 or halogen; R3 is II; optionally substituted C,-Csalkyl, C2-C6alkenyl, C2C6alkynyl, or C3-C7 cycloalkyl, halogen; OH or OR10; R4 is H, optionally substituted C1C6alkyl, C3-C6alkenyl, C3-C6alkynyl, C3-C7 cycloalkyl, aryl or heteroaryl, R5 is H or Optionally substituted C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl, or C3-C7 cycloalkyl; or R4 and R5 together form a 5 or 6-membered heterocyclic ring; and R7, R8, R9 and R10 are optionally substituted C1-C3alkyl, C2-C3alkenyl, C2-C3alkynyl, or C3-C7 cycloalkyl; are purine receptor, particularly adenosine receptor antagonists, useful for treatment of, inter alia, movement disorders such as Parkinsons disease.
CN102846605A Medicinal composition, as well as preparation process and application thereof The invention discloses a medicinal composition, which comprises the following components in parts by weight: 5 to 15 parts of amoxicillin, 1 to 5 parts of clavulanate potassium, and 1 to 5 parts of ambroxol hydrochloride. The invention discloses an application of the medicinal composition in preparing medicaments for treating animal respiratory infectious diseases, in particular for preparing porcine infectious pleuropneumonia and haemophilusparasuis. The invention also discloses a preparation method of compound amoxicillin soluble powder. The compound amoxicillin soluble powder comprises the following components in parts by weight: 5 to 15 parts of amoxicillin, 1 to 5 parts of clavulanate potassium, 1 to 5 parts of ambroxol hydrochloride, and 75 to 93 parts of glucosum anhydricum. The raw materials are uniformly mixed according to an equivalent incremental principle to obtain the compound amoxicillin soluble powder. The medicinal composition disclosed by the invention is reasonable and scientific in prescription, the bioavailability of amoxicillin can be increased compared with an amoxicillin preparation, the drug resistance is reduced, and the curative effect is improved.
US7238714 Analgesics; antiinflammatory agents; antiarthritic agents This invention provides a compound of the formula (I): wherein A represents a phenyl group or the like: B represents an aryl or the like: E represents a 1,4-phenylene group; R1 and R2 independently represent a hydrogen atom or the like: R3 and R4 independently represent a hydrogen atom or the like: R5 represents —CO2H or the like: R6 represents an alkyl group having from 1 to 6 carbon atoms or the like: X represents a methylene group or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
CN101773665A Reproductive protective agent facilitating human fertilization The invention belongs to the field of human reproductive health, and relates to reproductive protective agent facilitating human fertilization. The reproductive protective agent is divided into three independent formulas, and is used sequentially before, during and after having sex. The three formulas of the reproductive protective agent have different functions, can not only protect the integrity of vaginal mucosa of women, reduce the friction resistance and the mechanical damage to the male genitalia and the female reproductive tract caused by friction when being used together, but also can significantly increase the number of the left female reproductive tract local sperms, prolong the survival time of the sperms, enhance the movement activity of the sperms and protect the activity of the sperms so that the sperms are not killed by various local reproductive tract harmful factors, so as to achieve the purpose of improving the success rate of single fertilization.
US20090209496 Methods and compositions for enhancing the efficacy of rtk inhibitors This invention relates to methods for treating, preventing and/or managing cancer in a subject including enhancing the efficacy of a Receptor Tyrosine Kinase inhibitor (e.g., a small molecule RTK inhibitor, e.g., Sorafenib or Erlotinib) by administering to the subject a Vascular Disrupting Agent (e.g., a Combretastatin or derivative thereof) sequentially or simultaneously in combination with said RTK inhibitor. Pharmaceutical compositions comprising a combination of a RTK inhibitor and a VDA are also provided.
WO2008009212A1 A standardised extract and its use in the manufacture of a medicament The present invention refers to a medicament which activates gastrointestinal movement. The medicament consists essentially of Cucurbitacin D and one or more substances form the group including: Cucurbitacin A, Cucurbitacin B, Cucurbitacin E, Isocucurbitacin B and Isocucurbitacin D. The medicament is made from an extract obtained from Muskmelon Base, the fruit stem of Cucumis melo L. The medicament can promote enterokinesia in both normal animals and in animal models where gastrointestinal movement is inhibited. It has also been demonstrated to activate the movements of the stomach, small and large intestines. The extract may be used alone or in combination with the other botanical ingredients or chemical substances to form the pharmaceutical preparation.
WO2011015349A2 Methods for enhancing the cognitive function A compound having an affinity to a SV2 protein for the treatment of a condition associated with enhancement or improvement of the cognitive ability or to counteract cognitive decline of a mammal. For example, a compound which is covered by formula (I) R1 is an halogen atom, preferably, a chlorine or a fluorine atom; n is equal to 1, 2 or 3; and R2 is cyano.
US7235564 11'-substituted; potent inhibitors of cellular mitosis and proliferation The present invention relates to novel vinorelbine derivatives. Pharmaceutical compositions containing these compounds as well as processes of preparation and processes of use for treatment of various conditions are also disclosed.
CN101040987B Medicine for treating fever after cesarean section The invention discloses a medicament for treating postoperative pyrexia, wherein the raw material includes gupse, astragalus root, Chinese angelica root, rhizoma dioscoreae, white atractylodes rhizome, honeysuckle flower, dandelion and Bupleurum root.
CN102302551A Nose cleaning nursing liquid and preparation method thereof The invention discloses a preparation method of nose cleaning nursing liquid, which comprises the following steps: (1) weighing 500-2500 parts of raw material borneol camphor fresh branch and leaf by weight and 5-30 parts of sodium chloride; (2) putting the borneol camphor fresh branch and leaf in an extraction tank, slowly distilling by using water vapor and extracting distilled fliud; (3) standing the distilled fluid and waiting essential oil and water to layer, taking the water layer; (4) filtering the taken water layer, removing particles therein, and obtaining borneol liquid; (5) adding the weighed sodium chloride in the borneol camphor liquid obtained in the step (4), fully dissolving and blending, and obtaining borneol camphor mixed liquid; (6) detecting the borneol camphor content in the obtained borneol camphor mixed liquid and controlling not less than 0.6mg/mL; (7) sterilizing the detected borneol camphor mixed liquid and obtaining the nose cleaning nursing liquid. The nose cleaning nursing liquid is prepared by a distillation method, has a good effect in clinical tests, is safe, non-irritant, cool and refreshing does not have residues, toxicity and side effect, and achieves the effect of cleaning nasal cavities, and the improvement percentage of symptoms are is between 70 and 78.9 percent. In addition, the verities of the nose cleaning nursing liquid is enriched, so that patients are not limited to the conventional mint odor type nose cleaning nursing liquid.
CN103285034A Medicine for treating chilblain and manufacturing method thereof The invention belongs to the technical field of medicine chemical engineering, and particularly relates to a medicine for treating chilblain, which is characterized by comprising the following raw materials in parts by weight: 3-5 parts of iodine, 3-5 parts of potassium iodide, 8-12 parts of glycerol, 4-6 parts of lanolin, 4-8 parts of beeswax, 50-70 parts of vaseline, 1.5-5.5 parts of borneol, 0.5-1.5 parts of eugenol, 4-6 parts of methyl salicylate and 1-3 parts of sheep horn powder or ox horn powder or buckhorn powder with the fineness of less than 150 meshes. The invention also discloses a manufacturing method of the medicine for treating chilblain. The invention mainly has the advantages of simple manufacturing process, long storage time, short treatment time and low treatment cost, and is fragrant.
US20100204294 Methods For Assessing, Improving, Or Maintaining Urogenital Health in Postmenopausal Woman This invention relates to methods and kits useful for improving or maintaining urogenital health using an estrogen agonist/antagonist. The methods of treatment are effective for improving or maintaining urogenital health while substantially reducing the concomitant liability of adverse effects associated with estrogen administration. This invention also relates to methods of assessing vaginal health.
CA2158791C Dna sequences encoding the machado-joseph disease gene and uses thereof A method by which a nucleotide sequence, specifically a CAG triplet repeat shown to be expanded in individuals with Machado-Joseph Disease can be identified in a sample obtainable from an individual. The present methods can be used to identify individuals in whom the CAT triplet repeat is expanded, including methods useful to identify the protein encoded by the Machado-Joseph Disease gene.
CN102232938A Metaxalone capsule and preparation method thereof The invention relates to a metaxalone capsule and a preparation method thereof. The metaxalone capsule content comprises the following components: 20-60% of metaxalone, 20-40% of high molecular material, 5-20% of oil and fat, 10-20% of adsorbent and 0.1-1% of disintegrant. The metaxalone capsule prepared by the invention has the characteristics of high dissolution rate and high bioavailability.
EP2155681A1 Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof The invention relates to compositions comprising 2-(5-(4-(2- morpholinoethoxy)phenyl)pyτidin-2-yl)--V-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-<4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-ΛΛbenzylacetainide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention.
CN102079772A Pentacyclic triterpene-13,28-lactone compounds as well as preparation method and application thereof The invention discloses pentacyclic triterpene-13,28-lactones with antineoplastic activity, shown as a general formula I, or pharmaceutically acceptable salts thereof as well as a preparation method and medical application thereof, belonging to the field of biological medicines. The preparation method of the compounds, provided by the invention, has the advantages of mild reaction conditions, simplicity in operation, higher yield as well as strong practicability and structural universality. Shown by a pharmacologic test result, the compounds provided by the invention have favorable antineoplastic activity and can be applied as an antineoplastic drug in clinic.
WO2006079209A1 Pulmonary compositions comprising a vitamin a compound and a surfactant and uses thereof The current invention is directed towards a pulmonary composition comprising a vitamin A compound in combination with a pulmonary surfactant, wherein said vitamin A compound is miscible or soluble with said surfactant. The invention also provides a method of treating a pulmonary disorder by administering the pulmonary composition to the lungs of a subject (e.g., intratracheally).
WO2008031820A3 Combinations of class-i specific histone deacetylase inhibitors with proteasome inhibitors The present invention is concerned with combinations of a proteasome inhibitor and a class-I specific histone deacetylase inhibitor for inhibiting the growth of tumor cells, useful in the treatment of cancer.
US7053061 Vegetable oil phase containing dispersed Amphotercin B; water phase containing dissolved glycerin, mannitol, or dextrose tonicity modifiers; emulsifier such as natural phosphatides Parenteral compositions of oil-coated-Amphotericin B in structured-emulsion form, having LD50 of at least 400 mg/kg in mice and process for making the same have been described. The process essentially requires dispersing Amphotericin B in oily vehicle and dispersing emulsifier in the aqueous phase. The process of present invention is simple, cost effective and gives a stable product suitable for parenteral administration. Amphotericin B emulsion compositions prepared by the process of the present invention may be administered to human beings and animals for the treatment of fungal infections, with substantially equivalent or greater efficacy and low drug toxicity as compared to the conventional composition containing Amphotericin B and sodium desoxycholate.
EP1453810B1 Substituted 4-phenyltetrahydroisoquinolines, method for the production thereof, the use thereof as medicaments, in addition to a medicament containing same The invention relates to compounds of formula (I), wherein R1 - R9 which have the meaning as cited in the claims, are extremely suitable as antihypertensives for reducing or preventing ischemically induced injuries, as medicaments for operative intervention for the treatment of ischemics of the nervous system, strokes and swelling of the brain, shocks, disturbed respiratory functions, for the treatment of snorers, as a laxative, as agents against ectopic parasites, for the prevention of gallstones, as antiatherosclerotic agents, agents against diabetic late complications, cancer, fibrotic diseases, endothelial dysfunctions, organ hypertrophia and hyperplasia. Said compounds are also inhibitors of the cellular sodium-proton-antiporters, they influence serum lipoproteins and can be used in the prophylaxis of and for the regression of atherosclerotic alterations.
CN103203012A Joint health care product The invention discloses a joint health care product, which includes: N-acetylglucosamine, type II collagen and shark chondroitin. For the joint health product, shells of crabs shrimps and other carapace animals are added to undergo a natural fermentation process so as to obtain the N-acetylglucosamine, which has the advantages of good solubility, good stability, and good taste, etc. And as the N-acetylglucosamine is prepared by natural fermentation, compared with the chemosynthetic glucosamine hydrochloride or ammonia sulfate added in traditional joint health care products, it is in favor of absorption by the human body. Thus, the joint health care product is easy to absorb.
EP1937362A2 Bisphosphonate formulation A bisphosphonate for treatment of osteoporosis is formulated with an amount of an antifoaming agent effective for reducing foaming in the stomach, leading to reduced reflux and oesophageal irritation in use and increased patient compliance.
CN103356525A Application of Sarcaboside B in thrombocyte-increasing medicines The invention relates to new application of a compound Sarcaboside B in the field of pharmacy, particularly application of Sarcaboside B in preparing thrombocyte-increasing medicines. The application of Sarcaboside B in preparing medicines for treating low thrombocyte is disclosed for the first time. Since the framework type is brand-new and has unexpectedly high activity for inhibiting low thrombocyte, the Sarcaboside B does not has the possibility of any inspiration given by other compounds, has outstanding substantive characteristics, and obviously has significant progress in preventing and treating low thrombocyte.
CN103272081A Bony spur softening paste The invention relates to a bony spur softening paste which comprises raw materials in parts by weight: 15-25 parts of Chinese angelica, 15-25 parts of safflower, 25-35 parts of red paeony root, 15-25 parts of rhizoma drynariae, 35-45 parts of rheum officinale, 25-35 parts of szechuan lovage rhizome, 15-25 parts of jackinthepulpit tuber, 25-35 parts of radix aconiti preparata, 25-35 parts of prepared kusnezoff monkshood root, 20-30 parts of white mustard seed, 25-35 parts of Chinese wild ginger, 25-35 parts of tooth soap, 15-25 parts of notopterygium root, 15-25 parts of pubescent angelica root, 3-9 parts of mothball, 25-35 parts of Chinese yellow azalea, 25-35 parts of homalomena occulta, 15-25 parts of cortex Illicii, 25-35 parts of myrrh, 3-9 parts of borneol, 45-55 parts of piper wallichii, and 35-45 parts of kadsura pepper stem. The preparation method comprises the following steps: the components are processed according to the ancient processing in a way strictly controlling the quality; crushing, grinding and sieving by a 200-mesh basket together; taking raw medicinal powder 20 g, and adding honey to prepare a shape of the paste. The paste can not to be too dry, and is applied to an affected part externally, without flowing; the medicine is changed every three days, every 10 times are taken as a treatment course, and 2-3 treatment courses are required for few serious patients. According to the invention, the treatment course is short, the curative effect is obvious and side effect is avoided.
CN102335156A Etodolac double-layered osmotic pump controlled release tablets, and preparation method thereof The invention belongs to the field of medicines, and specifically discloses etodolac double-layered osmotic pump controlled release tablets, and a preparation method thereof. The etodolac double-layered osmotic pump controlled release tablets provided by the invention are double-layered tablets with semi permeable membranes. The upper layers of the tablets are medicine-containing layers comprising medicines and auxiliary materials, and the lower layers are assisting layers composed of polymers and osmotically active substances. The etodolac double-layered osmotic pump controlled release tablets provided by the invention have advantages of stable in vivo blood-drug level, and long effective blood-drug level duration.
WO2009010987A1 An improved process for the preparation of pure palonosetron hydrochloride The present invention relates to an improved and industrially viable process for the preparation of high purity >99.8% chemical and >99.8% chiral of palonosetron hydrochloride of formula-I ((3as)-2[(3s)-1-azabicyclo [2.2.2] oct-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinoline-1-one monohydrochloride) obtained from reduction of 2-[(S)-1-azabicyclo[2.2.2]oct-3-yl]-2,4,5,6-tetrahydro-1H-benz[de]iso-quinolin-1-one hydrochloride of formula-VI. In the prior art compound of formula-VI or its base are used in the catalytic hydrogenation. But the selection of solvents like acetic acid or THF rendered them commercially not viable due to low yield and low purity of palonosetron hydrochloride. In the present process simple solvent like methanol and readily available palladium-on-carbon were used to increase the yield and purity of palonosetron hydrochloride. Palonosetron Hydrochloride is useful as anti-emetic agent during the chemotherapy of treatment of cancer patients and is marketed under the brand names 'Aloxi' and 'Onicit'.
US20090324689 inhibiting the transition from the dry form of age-related macular degeneration to the wet form with rapamycin or analogs such as AP 23841, zotarolimus, tacrolimus, everolimus, pimecrolimus, temsirolimus; implants Diseases associated with the tissues in the posterior segment of the eye can be effectively treated by administering therapeutic agents transsclerally to those tissues. Compositions, devices, and methods for delivering therapeutic agents so that they cross the sclera and reach these tissues include injecting solutions or suspensions adjacent to or within the sclera and implanting solid structures containing the therapeutic agent adjacent to or within the sclera. These methods may be used for administering rapamycin or related compounds to treat choroidal neovascularization associated with age-related macular degeneration.
CN101054346A Preparation method and use for a set of novel compound and composition thereof The invention relates to a new compounds of (s)-2-(alpha-hydroxy pentyl) benzoate and preparation method therefor, and its application in medicines for treating and preventing cardio-cerebrovascular disease, aphrenia, cephalalgia, vertigo, acoasm and enhancing memorization etc, or medicinal composition containing activity component of present invention.
US20120101106 Tetrahydronapthyridine Orexin Receptor Antagonists The present invention is directed to tetrahydronapthyridine and tetrahydropyridopyrazine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
CN102532118A Indolone-containing 4-thiazolidone derivatives and application thereof The invention relates to indolone-containing 4-thiazolidone derivatives shown in a general formula I as well as geometrical isomers and pharmaceutically acceptable salts of the indolone-containing 4-thiazolidone derivatives. In the formula I, substituted groups namely Ar, R2, R3, R4 and n are defined in the specification. The invention also relates to application of compounds of the general formula I in preparation of a medicine for treating and/or preventing cancer.
WO2008116641A3 Oleyl phosphocholine The invention relates to the use of oleyl phosphocholine and oleyl-phospho-(N.N.-dimethyl-N-ethyl)-ethyl-ammonium for the long-term and continuous treatment of serious illnesses, such as cancer, leishmaniasis, ehrlichiosis, multiple sclerosis and psoriasis, in addition to other indications mentioned in the application.
WO2006072878A1 Oral dosage forms of sertraline having controlled particle size and processes for their preparation The present invention relates to pharmaceutical composition for oral administration comprising sertraline or pharmaceutically acceptable salts thereof in which the sertraline hydrochloride has a particle size of d?90#191 ranging from about 20 µm to about 40 µm and of d?50#191 ranging from about 5 µm to about 15 µm. The composition is bioequivalent to a reference pharmaceutical composition.
WO2013029198A1 Adefovir dipivoxil solid formulation and preparation method therefor An Adefovir Dipivoxil solid formulation and preparation method therefor. The method includes heating a pharmaceutical solvent and an inclusion agent for dissolution, leaving it for cooling to the room temperature, then mixing with Adefovir Dipivoxil, and suctioning the solvent to give Adefovir Dipivoxil granules, and further mixing with a pharmaceutical additive for uniform tableting or capsulation, wherein the Adefovir Dipivoxil granules are 0.5-3 parts, the pharmaceutical additive is 1-25 parts, and the Adefovir Dipivoxil granules comprise Adefovir Dipivoxil of 0.5-1 parts and the inclusion agent of 0.05-0.15 parts.
CN103071139A Combined crude herb moxibustion medicines for warming Yang to dispel cold and warming and activating meridians and collaterals and preparation method thereof The invention discloses a group of combined crude herb moxibustion medicines for warming Yang to dispel cold and warming and activating meridians and collaterals. The combined crude herb moxibustion medicines are characterized in that the combined crude herb moxibustion medicines are composed of the following materials: raw white mustard seeds, corydalis tubers, gansui roots, manchurian wildgingers, Sichuan lovage rhizomes, cowherb seeds, dried gingers, cinnamon, cassia twigs and borneol. The preparation method includes the following steps: the medicines, except the borneol, are ground into fine powder; the borneol is separately finely ground, the same amount of fine powder is added in the borneol powder, the mixed powder is screened by a 100-mesh screen and uniformly mixed, and therefore the combined crude herb moxibustion medicine is obtained. When in use, 5g of fine powder is adopted, 5ml of mature vinegar is added and mixed to form paste, the paste is produced into a medicinal cake for later use, and the medicinal cake is about 0.2cm to 0.3cm thick and about 1cm in diameter. The group of medicines have the functions of warming Yang to dispel cold and warming and activating meridians and collaterals. The group of medicines are mainly used for treating 'winter diseases' caused by the reinfection of wind-cold-wetness evil as the result of insufficient anti-pathogenic energy and Yang Qi exhaustion, such as asthma, senile chronic bronchitis, allergic rhinitis, arthralgia syndrome and pain in the neck, the shoulders, the waist and the legs, which can easily occur in winter but can be easily alleviated in summer.
WO2009127210A1 Vasodilating agents for the treatment of sleep attacks The present invention relates to at least one vasodilating agent, such as glyceryl trinitrate, for acute prevention or treatment of patients suffering from somnolepsy, a new sleep disorder characterized by somnoleptic seizures and/or sleep attacks, and acute treatment of sleep attacks in other known sleep disorders. The vasodilating agent has an onset of action within 15 to 60 seconds after administration and may thus prevent sleep attacks when a forewarning of a sleep attack is experienced. The effect of the vasodilating agent may be prolonged by further administrate an immediate release formulation comprising a CNS-stimulant, such as methylphenidate.
CN1969831A Capsule containing terramycin, oryzanol and vitamin for treating pharyngitis The invention discloses a triad pharyngitis capsule through three kinds of general purpose drug, which comprises the following parts: 80%-8 5% terramycin, 3%-4% oryzanol, 3%-4% vitamin B1 and 9%-11% auxiliary material (magnesium stearate or starch), wherein the drug powder is blended evenly, which is canned into 300 mg capsule.
US7223867 Preparation of benzosuberonylpiperidine compounds Diastereoselective and enantioselective synthetic routes for the preparation of compounds of formula (I): or derivatives thereof, wherein: R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, arylC1-6alkoxy, heteroarylC1-6alkoxy, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, arylC1-6alkylamino, heteroarylC1-6alkyamino; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 and R4 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl,(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6 alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo.
CN101700397B Tibetan medicine composite for treating diabetes and preparation method of preparation thereof The invention relates to a Tibetan medicine composite for treating diabetes, comprising the following components: 4.8-7.2g of medicine terminalia fruit, 2.4-3.6g of Chaxun ointment, 4-6g of long pepper extract, 3.2-4.8g of bright salt, 4.8-7.2g of trona, 2.4-3.6g of costustoot, 4-6g of fructus coriandri sativi, 2.4-3.6g of Tibet inula root, 4.8-7.2g of round cardamom, 4-6g of dried ginger, 2.4-3.6 cortex cinnamomi, 4-6g of red flower, 4-6g of savoury rhododendron leaf, 1.6-2.4g of pomegranate seed, 2.4-3.6g of rhubarb, 0.8-1.2g of purpurea halitium, 0.8-1.2g of flos caryophyllata, 4-6g of fructus terminaliae billericae, 1.6-2.4g of Shaji ointment, 2.4-3.6g of emblic leafflower fruit, 0.8-1.2g of crocus sativus, 0.8-1.2g of bear gall, 4-6g of fructus tsaoko, 4-6g of siberian solomonseal rhizome, 2.4-3.6g of puncturevine caltrop fruit, 4.8-7.2g of embelia laeta, 7.4-9.6g of herba dracocephali tangutici, and 7.4-9.6g of tinospora sinensis. The Tibetan medicine composite of the invention has significant clinical efficacy, little toxic and side effects and simple and convenient preparation.
WO2008140545A3 Inhibiting smad signaling promotes neuron regeneration Regeneration of a lesioned CNS axon of a mature neuron, determined to be subject to regeneration inhibition by Smad2/3 signaling, is promoted by contacting the neuron with an inhibitor of Smad2/3 signaling sufficient to promote regeneration of the axon.
US7056931 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods The current invention provides novel 2-substituted 1,2,3,4-tetrahydroquinolin-6-ols and derivatives thereof of the formula (I) (A); pharmaceutical compositions thereof, optionally in combination with estrogen or progestin; methods for inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
CA2783696A1 Use of compounds in the treatment or prevention of skin disorders Use compounds in the treatment or prevention of skin disorders The invention relates to the use of a compound of following formula (I) or one of its pharmaceutically acceptable salts, pharmaceutically acceptable solvates or hydrates in the preparation of a medicament intended to prevent and/or treat inflammatory skin pathologies.
WO2009038759A2 1-(4-(benzylbenzamid0) -benzyl) azetidine-3-carboxylic acid derivatives and related compounds as slp receptor modulators for the treatment of immune disorders The present invention relates to amides that have activity as SlP receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate SlP receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non- glomerular nephrosis, hepatitis, Behcet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
CN102836151A Application of Brevilin A when serving as JAK-STATs signal target inhibitor The invention provides a novel application of Brevilin A when serving as a JAK-STATs signal specific inhibitor. Cell model screening experiments and protein molecule detection prove that Brevilin A has excellent JAK-STATs signal inhibition activity, and can effectively inhibit expression of related genes, so that the growth of cells on which JAK-STATs signal rely can be effectively inhibited. Therefore, the Brevilina A serving as the active component can be used for preparing a medicament based on JAKs serving as a target spot or the JAK-STATs signals serving as a target, and treating diseases related to JAK-STATs signal activation; and various dosages of target medicaments can be prepared from the Brevilin A serving as the active component by adopting pharmaceutically acceptable process and auxiliary materials, such as various oral preparations, injections.
USRE42132 have special action with respect to tubulin polymerization inhibition and can be used for treating prostate cancer, breast cancer, colon cancer, non-small-cell-lung cancer, or primary dermal microvascular endothelial cell proliferation; 2-methoxy-17a-oxo-17a-homoestra-1,3,5(10)-trien-3-yl sulfamate This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for treating tumor diseases, which can be influenced positively by the inhibition of tubulin polymerization. The compounds according to the invention are distinguished by a D-homo-substitution. They have a special action with respect to tubulin polymerization inhibition and can be used, for example, for treating prostate cancer
US7632872 Providing analgesia in a newborn subject, the method comprising administering to the subject or to the mother a therapeutically effective amount of xenon In a first aspect, the present invention relates to the use of xenon in the preparation of a medicament for providing analgesia in a newborn subject and/or a fetal subject. In a second aspect, the invention relates to a method of providing analgesia in a newborn subject, the method comprising administering to the subject a therapeutically effective amount of xenon. In a third aspect, the invention relates to a method of providing analgesia in a fetal subject, the method comprising administering to the mother of the fetal subject a therapeutically effective amount of xenon for both the mother and fetal subject.
US8173160 Compositions comprising edible oils and vitamins and/or minerals and methods for making the compositions The invention provides compositions for an administration to a mammal orally or in a suppository that include one or more edible oils (preferably including one or more omega-3 fatty acids), one or more plant stanols, phytosterols, or esters thereof, and admixed in the one or more edible oils one or more water-soluble vitamins and/or minerals, for example, vitamins B6, B9 and/or B12. The invention also provides a method of making the compositions comprising mixing the foregoing components to form a suspension or emulsion of the vitamins and/or minerals in the edible oils. The mixture can be inserted into hollow soft or hard capsules, gelcaps or caplets. The edible oils can coat particles of the water-soluble vitamins and/or minerals, which may provide them with an improved absorption in the body due to an increased resistance to degradation in the acidic environment of the stomach.
CA2816679A1 3-(aminoaryl)-pyridine compounds The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are pharmaceutical compositions containing these compounds and methods of treating a disease or condition mediated by CDK9 using these compounds and compositions.
CN102793689A 2-methoxyestradiol dry powder inhalant serving as antitumor medicament and preparation method thereof The invention relates to a 2-methoxyestradiol dry powder inhalant serving as an antitumor medicament and a preparation method, which can be used for effectively solving the problems of poor oral administration effect and large administration dosage of 2-methoxyestradiol and short half-life period and the need of frequent administration in intravenous injection administration. According to the technical scheme for solving the problems, the 2-methoxyestradiol dry powder inhalant consists of the following components in percentage by weight: 50-90 percent of 2-methoxyestradiol, 0-5 percent of a flow aid, 5-50 percent of a thinner and 0-5 percent of a surfactant, wherein the flow aid is magnesium stearate or stearic acid; the thinner is one or a mixture of more than two of lactose, glucose, cane sugar and mannitol; and the surfactant is one of phospholipid, oleic acid and poloxamer. The antitumor medicament has the advantages of convenience in using, low administration dosage, small toxic and side effects, high stability, high safety and capability of directly reaching a focus, and is an innovation on a treatment means for treating tumors with 2-methoxyestradiol.
CA2721506A1 Compositions and methods for treating or preventing prostate cancer and for detecting androgen receptor variants The invention features diagnostic and therapeutic methods and compositions featuring androgen receptor variant proteins and nucleic acid molecules whose expression is increased in androgen related diseases or disorders.
US20080096832 non-nucleoside HIV-1 reverse transcriptase inhibitor (NNRTI); co-administering cytochrome P450 inhibitor such as ritonavir to reduce metabolism of the NNRTI 5,11-Dihydro-11-ethyl-5-methyl-8- {2-{(1-oxido-4-quinolinyl)oxy}ethyl}-6H-dipyrido[3,2-b:2',3'-e] [1,4]diazepin-6-one, (BILR 355 ) by half An improved method for using a NNRTI in the treatment of HIV-1 infection, comprising administering to a human, needing treatment for HIV-1 infection, a therapeutically effective amount of said NNRTI or a pharmaceutically acceptable salt thereof, and an amount of an inhibitor of the cytochromes P450 that is sufficient to elevate, enhance, or extend plasma concentrations of said NNRTI.
CN101336902A Liposomes sodium morrhuate The invention discloses a liposome-encapsulated sodium morrhuate, which is prepared from the following active ingredients (vol.%) sodium morrhuate 1-10, lecithin 4.31-10, cholesterol 0-2.19, vitamin E 0-0.03 and PBS buffer in balancing amount. The sodium morrhuate is used as an encapsulated active ingredient and is a sodium salt mixture of multiple fatty acids with eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) as main components, wherein the unsaturated fatty acids include from fatty acids with 18 carbon atoms and 3 olefinic bonds to fatty acids with 22 carbon atoms and 6 olefinic bonds. The liposome encapsulation technology completely solves the acute toxicity problem of sodium morrhuate used as a hardener, so that the drug has good passive targeted drug delivery function and reduced toxic and adverse effects caused after the drug enters the systemic blood circulation system. The inventive liposome-encapsulated sodium morrhuate can be used for treating hemangioma and vascular malformations.
CN101029038A Benzofurantone compound, its production and use A compound benzopyranone used for preparing the antineoplastic medicines is prepared from Dothiorella sp. HTF through seed culture, fermenting, filtering to obtain supernatant and thallus, extracting from thallus in methanol, collecting the extracting liquid vacuum concentrating to obtain petroether phase and water phase, extracting from the water phase in ethyl acetate, vacuum concentrating of organic phase, chromatography by silica gel column, gradient eluting with chloroform- methanol, and purifying by silica gel column.
CN101129728A Medicine for treating osteoproliferation The invention relates to a medicament for treating hyperosteogeny which is prepared from pubescent angelica root, notopterygium root, achyranthes and cyathula root, safflower, asaryl, prepared aconite root, pseudo-ginseng, notoginseng, Sichuan aconite root, Kusnezoff monkshood root, prepared aconite root, centipede, Clematis chinensis, wood louse, buck grass, boneol, camphor, frankincense, myrrh, toasted garlic, the herbs are immersed in vinegar for 2-5 days and can be applied onto the suffered positions through inunction.
EP2526935A1 Hydrazidomycins The present invention relates to pharmaceutical formulations comprising specific hydrazidomycin compounds. Since said hydrazidomycin compounds show cytotoxic activities, the present invention further relates to said hydrazidomycin compounds for use in medicine, in particular in the treatment of proliferative disorders.
EP2138173A1 Pharmaceutical compositions comprising aminoadamantane derivatives The present invention relates to pharmaceutical compositions comprising 1-aminoadamantane derivatives and a cyclodextrin, which compositions exhibit advantageous safety, convenience, and dosing characteristics. The compositions of the instant invention find particular application in the treatment of various diseases and conditions of the CNS, including those involving the impairment of cognitive function or dementia, such as Alzheimer's disease.
WO2006093823A1 2- [ isoquinolin-s - carbonyl ) amino] -propionic acid derivatives as inhibitors of factors xi and ix for the treatment of thrombosis This invention provides aryl and heteroaryl compounds of formula (X). The compounds of the invention may be useful as antagonists, or partial antagonist of factor IX and/or factor Xl and thus, may be used to inhibit the intrinsic pathway of blood coagulation. Formula (X) wherein R102 is selected from the group consisting of -C(O)OH, -C(O)OCH3, -C(O)O-t-butyl, -C(O)NH-OCH2-phenyl, C(O)NHOH, and -C(O)NHSO2CH3; and wherein R101 .R103,R104 and Y are as defined herein.
CN101856327A Aerosol with quantitative inhalation of bencycloquidium bromide and preparation method thereof The invention discloses an aerosol with quantitative inhalation of bencycloquidium bromide and a preparation method thereof. The aerosol can be used for a non-freon (CFC) solution type formula which has high fine particle fraction (FPF). Shown by pharmacokinetic test results, the aerosol has fast effect, can be used for treating asthma and chronic obstructive pulmonary disease (COPD) and has good antiallergic function.
CN1785166A Method for quality control of infantile amfenac alkylamine A quality control method for the infantile Anfenwanan medicine includes examining its characteristics, the identification to acetylaminophenol and artificial ox gallstone, examining the content uniformity of chlorphenamine maleate, and measuring the contents of acetylaminophenol, coffeine, chlorphenamine maleate and mydantane.
US20110130448 Functionalized phenolic esters and amides and polymers therefrom The present invention relates to a compound of the formula: R-AR—O—Y—R′ Wherein R represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid, —NO2, —NH2, —NHCOCH3, and —NH—Y—R′, which is attached directly to AR or attached through an aliphatic chain. The carboxylic acid moiety in R includes but is not limited to the following carboxylic acids: benzoic acids, cinnamic acids, ferulic acid, caffeic acid, syringic acid, salicyclic acid, vanillic acid, phenylacetic acids, phenylpropionic acids, and sinapinic acid. -AR—O— is a biologically active phenolic moiety comprising 1 to 6 substituted or unsubstituted aryl rings that are directly bonded to each other, fused together, or joined through a linking group. Y represents a member selected from: —COCH2O— (glycolic ester moiety) —COCH(CH3)O— (lactic ester moiety) —COCH2OCH2CH2O— (dioxanone ester moiety) —COCH2CH2CH2CH2CH2O— (caprolactone ester moiety) —CO(CH2)mO— where m is an integer between 2-4 and 6-24 inclusive —COCH2—O—(CH2CH2O)n— where n is an integer between 2 and 24, inclusive; and R′ is either hydrogen or a benzyl or an alkyl group, the alkyl group being either straight-chained or branched. The resultant functionalized phenolic compounds, used singly or in combinations, and their polymers have controllable degradation profiles, releasing the active component over a desired time range. The polymers are useful for biomaterials and biomedical devices, wherein said biologically active phenolic moiety is a residue of a phenolic compound.
CN102106812B Azithromycin ultrafine powder in-situ gel eye drops and preparation method thereof The invention provides azithromycin ultrafine powder in-situ gel eye drops and a preparation method thereof. The method comprises the following steps of: firstly, micronizing a medicament by using a proper method to remarkably improve the dissolution rate and solubility of the medicament; and secondly, preparing an ophthalmic preparation which is in a liquid state in vitro and is in a gel state when dripped into eyes by adopting sodium alginate as an ion-sensitive gel matrix or adopting poloxamer 407 and poloxamer 188 as thermosensitive gel matrixes. The eye drops are steady in storage at 4 DEG C and uniform in content, and are not required for secondary preparation so as to reduce contamination. In the method, azithromycin ultrafine powder and in-situ gel are combined for the treatment of bacterial keratitis and trachoma; and by the dual effects of the ultrafine powder and the gel, the sustained release effect is achieved when the retention time of the preparation in the eyes is prolonged, so that the local bioavailability of the medicament and the compliance of patients are improved, and the medicament absorption of the cornea is increased to reduce the toxic or side effect caused by the systemic absorption of ophthalmic medicaments.
US20110177167 Hydrophilic/Lipophilic Polymeric Matrix Dosage Formulation An oral dosage form comprising a pharmaceutical tablet of one or more layers, one of which carries a biologically active substance; the formulation of said tablet includes different percentages of hydrophilic and lipophilic polymeric materials, and adjuvant substances. The tablets of the present invention show a release rate which is independent from the amounts of active substance present in the tablet.
US20100255104 Pharmaceutical formulation of taxane A pharmaceutical formulation of taxane to be administered to mammals, preferably humans, including two compositions which are combined prior to their administration, forming a transparent solution free from precipitates and essentially free from foam, wherein said compositions comprise a solid composition of taxane and a solubilizing composition of said solid taxane composition comprising a tensoactive and an antifoam agent. A kit for such a formulation of injectable taxane includes a prefilled syringe. Also there is a pharmaceutical taxane perfusion solution.
CN102755312A Application of compound with flavone skeleton structure as Parkinsonism treating medicine The invention relates to application of a compound with a flavone skeleton structure as a Parkinsonism treating medicine. The compound with a flavone skeleton structure is an inhibitor for the catechol methylation transferase; and the compound specifically comprises radix scutellariae, scutellarein and structure derivatives of radix scutellariae and scutellarein, and can be used as a synergist of the Parkinsonism treating medicine levodopa. In-vitro activity test indicates that IC50 of the compound in inhibiting catechol methylation transferase can reach nanomole level, wherein the COMT(Catechol O Methyl Transferase) inhibition activity of scutellarein and the derivatives of scutellarein is superior to that of medicine tolcapone on the market. The rat overall pharmacokinetic study shows that by the joint application of scutellarein and levodopa, the blood concentration of levodopa can be obviously increased. Moreover, the compound does not generate active intermediate through metabolism activation or form toxic adduct together with biological macromolecules, thus the hepatotoxicity and nephrotoxicity caused by metabolism activation are avoided, and the compound has good prospect of patent medicine.
WO2008071456A3 3-h-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same The invention relates to 3-H-pyrazolopyridines according to the general formula (I) in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said 3-H-pyrazolopyridine compounds, to methods of preparing said 3-H-pyrazolopyridines, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said 3-H-pyrazolopyridines, as well as to uses of said 3-H-pyrazolopyridines for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
CN103655474A Compound drug-carrying liposome as well as preparation method and application thereof The invention discloses a compound drug-carrying liposome as well as a preparation method and application thereof. The compound drug-carrying liposome comprises a long-circulating liposome and medicinal active ingredients coated by the long-circulating liposome, wherein the long-circulating liposome is a liposome of which the surface is modified by distearoyl phosphoethanolamine-methoxy polyethylene glycol 2000; the medicinal active ingredients refer to anthracycline antibiotics and resveratrol. The preparation method of the compound drug-carrying liposome comprises preparing a liposome source, the distearoyl phosphoethanolamine-methoxy polyethylene glycol 2000 and the medicinal active ingredients into the compound drug-carrying liposome, wherein the medicinal active ingredients refer to anthracycline antibiotics and resveratrol. The compound drug-carrying liposome disclosed by the invention has inhibitory activity on the development of drug-sensitive tumors, can effectively inhibit the development of chemotherapeutic drug-tolerant tumors and is small in side effect, thereby achieving a great clinical application value.
WO2008038600A1 1,4-benzodiazepine derivative, pharmaceutical composition comprising the same, and use of the same for medical purposes A 1,4-benzodiazepine derivative having an [(R)-1-(2-chloro-4-alkoxybenzoyl)-3-methyl-1,2,3,5- tetrahydrobenzo[e]-1,4-diazepine-4-carbonyl]amine skeleton, such as methyl=(S)-2-[[(R)-1-(2-chloro-4-ethoxybenzoyl)-3- methyl-1,2,3,5-tetrahydrobenzo[e]-1,4-diazepine-4- carbonyl]amino]propionate or methyl=(S)-2-[[(R)-1-(2-chloro- 4-propoxybenzoyl)-3-methyl-1,2,3,5-tetrahydrobenzo[e]-1,4- diazepine-4- carbonyl]amino]propionate. The derivative has a V2 receptor-stimulating activity and is therefore useful as a prophylactic or therapeutic agent for central diabetes insipidus, nighttime urinary frequency or nocturnal enuresis.
WO2010046910A1 Pharmaceutical compositions for the treatment of diabetes mellitus Disclosed herein is a pharmaceutical composition comprising Hydroxychloroquine or its pharmaceutically acceptable salt and at least one antidiabetic compound, useful in the treatment of diabetes mellitus.
US20120035237 Pyrazole and triazole carboxamides as crac chann el inhibitors The present invention relates to amide compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing these compounds and to their use in therapy.
CA2128706C Polyunsaturated fatty acid based drugs, in particular docosahexaenoic acid, as platelet aggregation inhibitors and against essential fatty acid deficiencies of the brain Novel essential fatty acid based drugs comprising a substantial proportion of docosahexaenoic acid (DHA) in the class of fatty acids esterified in position sn-2 of phosphatidylcholines (PCDHAs) acetylated in position sn-1, or lysophosphatidylcholines (lyso-PCDHAs), or DHA-triglycerides esterified in position sn-2 and acetylated in positions sn-1 and sn-3. Said drugs are useful for treating cardiovascular diseases, including atheromatous disease, and essential fatty acid deficiency, particularly in the brain.
WO2006090616A1 Fat cell differentiation regulator [PROBLEMS] A novel partial agonist of PPARϜ, or the like, being useful for prevention/remedy of diseases caused by abnormal differentiation of fat cells; a method of activating PPARϜ by the use thereof; a method of prevention/remedy of diseases caused by abnormal differentiation of fat cells; etc. [MEANS FOR SOLVING PROBLEMS] The compounds of the general formula: (I) (wherein R1 and R2 are each a hydrogen atom, an alkyl, phenyl, benzyl or a functional group of the following formula (II) or formula (III) and may be identical with or different from each other) (wherein R3 is a hydrogen atom, a halogen atom, nitro, hydroxyl, an alkoxy or amino) are partial agonists of PPARϜ and are useful in the activation of PPARϜ and the prevention/remedy of diseases caused by abnormal differentiation of fat cells.
US7683052 Crystalline polymorph of bazedoxifene acetate The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.
WO2009117769A1 Inhibition of c-kit cancers The invention relates to a method for inhibiting c-KIT in a cancer cell, comprising treating the cancer cell with an agent for up regulating protein phosphatase 2A (PP2A) activity in the cancer cell. The agent can be an activator of PP2A such as FTY720. The inhibition of c-KIT can inhibit growth of cancer cells and has application in the prophylaxis or treatment of c-KIT cancers. Typically, the cancer is a non- leukemic cancer.
WO2009084970A1 5-o-substituted 3-n-phenyl-1,3,4-oxadiazolones for medical use The present invention relates to compounds having a 5-O-substituted 3-N-phenyl-1,3,4-oxadiazolone structural unit which have unexpectedly high level of inhibition of FAAH (fatty acid amide hydrolase). (I)
CN101333524B Small molecule noncoding RNA gene hsa-mir-101 and antineoplastic use thereof The invention discloses a small-molecular RNA gene hsa-miR-101 relevant to a primary hepatocellular carcinoma as well as an application thereof. The invention also provides a method for analyzing thecorrelation between the small-molecular RNA gene and the tumor formation and development, as well as purposes of the small-molecular RNA gene hsa-miR-101 at the aspect of primary liver cancer treatment. The invention aims to provide the small-molecular RNA gene hsa-miR-101 acting as the application of tumor therapeutic drugs, and has great practical significance and broad applying prospect in themedical and biopharmaceutical fields.
US20080293786 Novel 2-imino-1,3-thiazoline-based compounds and t-type calcium channel inhibitors containing the same Novel 2-imino-1,3-thiazoline based compounds represented by Chemical Formula I, and T-type calcium channel inhibitors containing the compound are provided. The T-type calcium channel inhibitors according to the present invention are useful as a treating agent of diseases associated with over-expression of the T-type calcium channel.
CN102014861A Moisturizing agent Disclosed is a moisturizing agent comprising a copolymer represented by formula (1). [In formula (1), A represents a substituent containing an oligosaccharide composed of 2 to 6 monosaccharide molecules bound to each other; B represents a group represented by formula (2); m and n represent numbers which meet the following equation m:n = 9:1 to 1:9; and Z represents a hydrogen group, a methyl group or an ethyl group.] [In formula (2), X represents a saturated or unsaturated monocyclic or dicyclic ring having 5 to 10 ring-constituting members, or a molecule containing a nitrogen or an oxygen, provided that the ring may contain 1 to 3 atoms independently selected from the group consisting of a nitrogen, a sulfur and an oxygen; n represents a number of 0 or 1; Y represents -NHCO-, -CONH-, -NHCONH-, -NH-, -CO, or an alkyl group having 0 or more carbon atoms; and R represents a linear or branched alkyl, alkenyl or alkynyl having 1 to 20 carbon atoms which, if required, may be substituted by one or two hydroxy, mercapto, amino, cyano, heterocyclyl, heterocyclyloxy, phenyl, benzyl, heteroaryl, phenoxy, benzyloxy or heteroaryloxy groups].
CA2256413C Anti-endoglin monoclonal antibodies and their use in antiangiogenic therapy A monoclonal antibody, or fragments thereof, having binding specificity for both endoglin expressed on proliferating human vascular endothelial cells and on proliferating murine endothelial cells. Antiangiogenic therapy in mammals can be effected by administering to the mammalian host a therapeutically effective amount of an anti-endoglin monoclonal antibody, or fragments thereof, which is conjugated to at least one angiogenesis inhibitor or antitumor agent. The composition is useful for treating tumor and angiogenesis-associated diseases.
CN102166360A Ibuprofen intravenously administrable preparation and preparation method thereof The invention provides an ibuprofen intravenously administrable preparation and a preparation method thereof. The injection comprises 0.4-4mg/ml of ibuprofen, an alkali regulator for regulating the pH value to 6.5-9.0 as required, 0.70-0.90wt%/volume of sodium chloride and water for injection.
CN101869545A Preparation method of embedded drug-loaded glucomannan and xanthan gum composite gel The invention relates to a preparation method of embedded drug-loaded glucomannan and xanthan gum composite gel, comprising the following steps of: dissolving levodopa or 4-amino salicylic acid with diluted hydrochloric acid aqueous solution; mixing konjac glucomannan (KGM) and xanthan gum (XG) with stock solution and then swelling; stirring for 1-3h at the room temperature; heating for 1-3h in a 75-90 DEG C water bath kettle; then cooling to the room temperature. The invention limits the releasing position of oral drugs and restrains the initial releasing speed of the drugs to realize colon targeting drug delivery and drug slow release by utilizing the characteristic that the matrixes KGM and XG of the composite gel can not be degraded in upper gastrointestinal but only can be graded at the position of he colon under the condition of flora and pH environment and the property that the two models of drugs can form the high-strength gel with the glucomannan/the xanthan gum through the mutual effect hydrogen bonds. The invention has mild preparation conditions, simple process and low energy consumption and is a safe environment-friendly preparation method.
CN102821770A Anti-viral formulations The present disclosure relates generally to the field of anti-viral therapy and prophylaxis. Formulations and agents are provided which inhibit viruses of the Orthomyxoviridae family and ameliorate symptoms and conditions caused by viral infection. The present disclosure teaches the control of influenza virus infection and spread and amelioration of conditions caused thereby. The formulations and agents may be processed as medicaments or as health supplements for more general application such as in the form of consumer goods or consumer foods.
CN1965864A Pharmaceutical composition for treating white lesions of vulva, formulation and preparation process thereof The invention discloses a pharmaceutical composition for treating white lesionsofthevulva, the preparation and the process for preparing same, wherein the pharmaceutical composition comprises the following raw materials (by weight portion): pearl powder 40-60 parts, concentrated hyocholic acid liquid 40-60 parts, borneol 5-15 parts, allume 5-15 parts, wherein the pearl powder comprises the following raw materials (by weight portion): calcined gypsum 50-80 parts, red halloysite 80-120 parts, calcined abalone shell 700-900 parts, dragon's bone 100-200 parts, borneol 20-40 parts, musk 5-15 parts, and pearl powder 5-15 parts.
WO2008063202A3 Heterobicyclic thiophene compounds for the treatment of cancer Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
US20080255230 Pain therapy; muscular disorders; diarrhea Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
EP1227859B1 Neurophilin ligands for treating ocular conditions The use of neurophilin ligands for treating glaucoma and lowering IOP is disclosed.
WO2004108715A8 3-aryloxy and 3-heteroaryloxy substituted benzo(b) thiophenes as therapeutic agents with pi3k activity The present invention provides benzo[b]thiophenes of Formula (I), wherein R1, R2, R3, R4, R5, and L have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (I).
CN102166204A Pharmaceutical composition for preventing and/or treating bone loss The invention provides a pharmaceutical composition which comprises an effective dose of bergapten and pharmaceutically acceptable carriers or excipients, and the pharmaceutical composition can be used for preventing and/or treating bone loss.
CN101472572B Use of a RAR antagonist or inverse agonist for the treatment of chemotherapy and/or radiation therapy side effects A method for treating chemo therapy or radiation therapy side effects in a mammal undergoing chemotherapy and/or radiation therapy, the method comprising a step of administering to the mammal a therapeutically effective amount of a RAR antagonist or RAR inverse agonist which binds to receptors of the RARalpha, RARbeta and RARgamma subtypes is disclosed. Such side effects include chemoradiotherapy-induced alopecia, chemoradiotherapy-induced thrombocytopenia, chemoradiotherapy-induced leucopenia and chemoradiotherapy-induced neutropenia.
US20050107317 Nucleic acid molecule of the short-chain dehydrogenase gene family, an antibody, an aptamer or receptors, polypeptide encoded thereby; biodrug for treatment of metabolism of triglycerides, metabolic disorders as obesity, eating disorder, cachexia, diabetes mellitus, hypertension, heart disease The present invention discloses CG3842 or SCAD homologous proteins regulating the energy homeostasis and the metabolism of triglycerides, and polynucleotides, which identify and encode the proteins disclosed in this invention. The invention also relates to the use of these sequences in the diagnosis, study, prevention, and treatment of metabolic diseases and disorders.
CN103705482A Preparation method of tiopronin tablets The invention relates to a preparation method of tiopronin tablets. The method comprises the following steps: (1) pelleting auxiliary materials, namely adding a diluent and a disintegrating agent into a binder, and pelleting the mixture by adopting a wet process; (2) drying and finishing pellets; (3) adding raw material tiopronin and additional auxiliary materials, and mixing; (4), tabletting to form tiopronin blank tablets; and (5) coating to form the tiopronin coated tablets. According to the preparation method of the tiopronin tablets, which is provided by the invention, the auxiliary materials, the diluent and the disintegrating agent are pelleted with the binder and are dried, and the raw material tiopronin and the additional auxiliary materials are added, mixed and tabletted, therefore, active ingredients in tiopronin can be protected against destroy due to wet and heat in a traditional wet method pelleting process, good stability of the tiopronin tablets is kept, and the problem that the traditional wet method pelleting process is not suitable for producing the tiopronin tablets is solved. The prepared tiopronin tablets are low in production cost, and the preparation operation is simple.
US8207194 Compounds having a 4-pyridylalkylthio group as a substituent A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is benzene or an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.
CN1927204A Pharmaceutical composition of ligustrazine and carthamus tinctorius yellow color Disclosed is a pharmaceutical composition and its preparing method and use thereof, wherein the composition comprises ligustrazine or its pharmaceutically acceptable salts and carthamus tinctorius yellow color, the range of the weight ratio of the two ingredients is 1:0.01-50, the two ingredients can be used individually or mixed with medicinal auxiliary materials so as to prepare clinically and pharmaceutically acceptable dose forms such as injections, constant release oral dosage forms, slow release and controlled release dosage forms, granules, pills and oral liquid preparations.
US20100324027 Diazahomoadamantane derivatives and methods of use thereof The invention relates to compounds that are diazahomoadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
US20110086073 NANOMETER-SIZED PRODRUGS OF NSAIDs The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of α-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.
WO2009140448A1 Tetrahydrocyclopenta[b]indole androgen receptor modulators The present invention provides a compound of the Formula (I), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating or preventing physiological disorders, particularly reduced bone mass, osteoporosis, osteopenia, reduced muscle mass or strength, or erectile dysfunction comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
EP1311488B1 Substituted imidazoles as tafia inhibitors The present invention provides compounds of formula (I). These compounds are a class of TAFIa inhibitors, atherosclerosis, adhesions, dermal scarring, cancer, fibrotic conditions, inflammatory diseases and those conditions which benefit from maintaining or enhancing bradykinin levels in the body.
CA2760106A1 Inhibitors of sialidase or sialidase-like enzymes The present invention describes compounds of Formula I (see formula I) or a pharmaceutically acceptable salts or derivatives thereof. Compositions comprising compounds of Formula I are also described. The present invention further relates to a method of producing non-2-enonate compounds.
US20120208778 Avermectins and milbemycins for the treatment, prevention or amelioration of flavivirus infections Avermectin and milbemycin compounds, particularly the substance ivermectin, for preparing an antiviral medicament for the treatment, prevention or amelioration of a Flavivirus infection, such as those caused by YFV (yellow fever virus), DENV (Dengue virus), JEV (Japanese encephalitis virus), TBEV (tick-borne encephalitis virus) or MODV (Modoc virus) are provided. The antiviral compositions of the present invention are suitable for oral administration to a Flavivirus-infected subject or a subject at risk of a Flavivirus infection, such as a human or other mammal.
CN102875632A Ursolic acid ester derivatives and preparation methods and applications thereof The invention discloses ursolic acid ester derivatives and preparation methods and applications thereof. Compound structures of the ursolic acid ester derivatives are respectively shown by the following formula (I) and formula (II). The invention is characterized in that the ursolic acid ester derivatives are synthetized by taking ursolic acid, halohydrocarbon, secondary amine and succinic acid as raw materials through at least two steps of substitution reaction. The ursolic acid ester derivatives can be used for preparing anti-cancer drugs.
WO2007116074A1 Trimetazidine for use in the treatment of fibromyalgia syndrome and related conditions The present invention provides a method for treating certain rheumatic conditions such as fibromyalgia syndrome, chronic fatigue syndrome, myofascial pain syndrome, and Gulf War syndrome, among others, by administration of trimetazidine, along with related compositions and kits.
CN102366317A Eye-protection wet tissue The invention relates to the field of wet tissues, in particular to an eye-protection wet tissue. Vitamin B6 and vitamins E have moisture keeping and nourishing functions. Dipotassium glycyrrhizinate is an antiallergic substance. Naphazoline hydrochloride is a decongestant drug. Chlorpheniramine maleate is an antiallergic drug. The wet tissue made of a hydro-entangled non-woven fabric is soft in texture.
US7019147 E.,g.,1-[2-(5-Methoxy-benzoimidazol-1-yl)-quinolin-8-yl]-piperidin-4-ylamine; anticarcinogenic and -tumor agent; KDR tyrosine kinase inhibitors; (KDR=kinase inserrt domain recepter) The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R7, R8, R9, R10, and R11 are as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1).
US7449487 In particular of avocado, soya bean and/or lupin oils, for preparation of a medicament intended to stimulate expression of TGF-62 or expression of the plasminogen activator inhibitor PAI-1 The invention relates to the use of at least one unsaponifiable component of vegetable oil, in particular of avocado, soya bean and/or lupin oils, for the preparation of a medicament intended to stimulate the expression of TGF-β or the expression of the plasminogen activator inhibitor PAI-1. The invention also relates to a method of cosmetic treatment comprising the application of at least one unsaponifiable component of vegetable oil as well as the use of the latter as additive in a food for human beings and/or for animals.
CN1562045A Doxycycline dripping pill A dripping pill of doxycycline for treating multiple inflammations, syphilis, gonorrhea, or chlamydia or mycoplasma injection is prepared from doxycycline or its salts or hydrates, and pharmacologically acceptable auxiliaries including non-ionic surfactant (polyethane glycol).
EP2235031A2 Synthesis of novel neamine derivatives and use thereof as antibacterial agents The invention relates to compounds of the formula (I) in which: R1 = OH or NH2; OR2, OR3, OR4 and OR5 form alcohol, ether, ester, carbonate, carbamate, sulphonate or sulphamate functions; and if R5 = H, if R2 =R3=R4, then R2, R3 and R4 ≠ H; if R2 = H, then R3 ≠ H and R4 ≠ H; if R3 = H, then R2 ≠ H and R4 ≠ H; if R4 = H, then R2 ≠ H and R3 ≠ H; if R5 ≠ H, if R2 = H, then R3 ≠ H and R4 ≠ H; if R3 = H, then R2 ≠ H and R4 ≠ H; if R4 = H, then R2 ≠ H and R3 ≠ H. The invention also relates to the use thereof as antibiotic agents and to a method for their synthesis.
CN101791296A Orlistat tablets and preparation method thereof The invention belongs to the technical field of the medicament and in particular relates to tablets comprising orlistat and a preparation method thereof. Orlistat and cyclodextrin which are subjected to enclosing and auxiliary materials acceptable for pharmacy are pressed into the tablets. The tablets solve the sticking problem of carrying out pressing on the orlistat by the conventional process, obviously improve the chemical and physical stability of the orlistat, cover the unpleasant taste of the orlistat, improve the administration compliance of the dysphagia patients, have good dissolution and improve the curative effect of the orlistat.
WO2009027644A3 Compositions for the treatment of neoplastic diseases Pharmaceutical compositions and methods for the treatment of neoplastic disease and comprising the combination of a taxane, such as docetaxel, with a CYP3A4 inhibitor, such as ritonavir. Methods of treatment of neoplastic disease incorporating the administration of a taxane and the administration of a CYP3A4 inhibitor, either simultaneously or separately, are also included. Further, kits for carrying out the methods are included. Solid pharmaceutical taxane compositions for oral administration comprising a substantially amorphous taxane, a carrier and a surfactant are also included.
WO2007116106A1 Novel compounds as antagonists of adenosine a1 receptors Compounds of formula (I), in which R1 represents an aryl or heteroaryl group optionally substituted by one or more substituents selected from halogen, optionally substituted linear or branched lower alkyl, cycloalkyl, hydroxy, optionally substituted linear or branched lower alkoxy, -SH, optionally substituted linear or branched lower alkylthio, cano, -NR'R', -CO2R'; -R2 represents a group selected from -CO(CH2)nR3, -CO(CH2)nN(R4)R3, - COO(CH2)nR3 and -(CH2)nR3; in which n is 0, 1 or 2; R3 represents a group selected from: a) an optionally substituted monocyclic or polycyclic heteroaryl or aryl group or b) a lower, linear or branched alkyl or cycloalkyl group, which is optionally substituted; and -R4 represents a hydrogen atom or optionally substituted linear or branched lower alkyl group; they are useful for treating a pathological disorder or disease likely to be improved by antagonism of the adenosine A1 receptor.
CN101057866A Method for preparing 'kelike' capsule The invention discloses a process for preparing compound paracetamot and amantadine lydrochloide capsules for treating common cold, wherein each tablet of the compound paracetamot and amantadine lydrochloide capsules comprises acetaminopher 250mg, amantadine hydrochloride 100mg, artificial ox gallstone 10mg, caffeine 15mg, chlorpheniramine maleate 2mg.
US20100292316 Improved therapeutic methods and compositions comprising chroman ring compounds The instant invention concerns chroman ring derivative compounds such as vitamin E derivatives and methods for their use. In certain aspects, methods for treating subjects comprising Arg, JNK, p73, NOXA or FOXO1 positive cancers are provided. In still further aspects, methods for treating cell proliferative disease such as cancer by administration of a chroman ring compound in conjunction with a P13 or Akt kinase inhibitor are described.
DE102005020105A1 New thiazolidinone compounds are polo-like kinase inhibitors, useful for the preparation of medicament to treat e.g. cancer, autoimmune disease, cardiovascular disease stenosis and infection disease Thiazolidinone compounds (I) and their solvates, hydrates, stereoiosomers, diasteromers, enantiomeres or salts are new. Thiazolidinone compounds of formula (I) and their solvates, hydrates, stereoiosomers, diasteromers, enantiomeres or salts are new. Q : aryl; A, B1>H, halo, OH, NR3>R4>, CN, NO2, 1-4C-alkyl, 1-6C-alkoxy, 3-6C-heterocycloalkyl (optionally substituted by halo, OH, 3-6C heterocycloalkyl, NR3>R4> or CO(NR3>)-M), (where the heterocycloalkyl contains one or more N, O, S, where -(CO)-, SO2 or double bonds in the ring is optionally interrupted, where the ring is optionally substituted with 1-6C-alkyl, 3-6C-cycloalkyl, 1-6C-hydroxyalkyl or NR3>R4>), NR3>(CO)-L, -NR3>(CO)-NR3>-L, COR6>, -O-(CH2)pR6>, CO(NR3>)-M, NR3>(CS)NR3>R4>, NR3>SO2-M, SO2-NR3>R4>, SO2(NR3>)-M or O-(CH2)p-aryl; p : 0-4; L : 1-6C-alkyl, 3-6C-heterocycloalkyl (optionally substituted with NR3>R4>), 1-6C-hydroxyalkoxy, 1-6C-dialkoxy or 3-6C-heterocycloalkyl, where the heterocycloalkyl contains one or more N, O, S, where -(CO)-, SO2 or double bonds in the ring is optionally interrupted, where the ring is optionally substituted with 1-6C-alkyl, 3-6C-cycloalkyl, 1-6C-hydroxyalkyl or NR3>R4>; M : 1-6C-alkyl (substituted with NR3>R4> or 3-6C-heterocycloalkyl); R1>1-4C-alkyl (optionally substituted with halo, 3C-cycloalkyl, allyl or propargyl); either R2>H or 1-6C alkyl, 1-6C alkoxy, 1-6C alkenyl, 1-6C alkynyl, 3-6C cycloalkyl, 3-6C heterocycloalkyl, aryl or heteroaryl (all optionally substituted with halo, OH, CN, 1-6C alkyl, 1-6C alkoxy, 1-6C hydroxyalkyl, 3-6C cycloalkyl, 3-6C heterocycloalkyl, 1-6C alkynyl, aryloxy, (hetero)aryl or with a group of -S-1-6C alkyl, -COR6>, -NR3>R4>, -NR3>(CO)-L or -NR3>COOR7>), where the heterocycloalkyl is optionally interrupted by one or more N, O or S atoms and/or optionally one or more -(CO)- or -SO2- group in the ring are interrupted and/or optionally one or more double bonds in the ring, and the (hetero)aryl, 3-6C cycloalkyl or 3-6C heterocycloalkyl ring in each case optionally substituted with one or more CN, halo, OH, 1-6C alkyl, 1-6C hydroxyalkyl, halo substituted 1-6C alkoxy, 3-6C cycloalkyl, 3-6C heterocycloalkyl, benzyl or (hetero)aryl; or R2>R5>3-6C heterocycloalkyl ring interrupted by at least one nitrogen and optionally interrupted by one or more O or S, or -(CO)- or -SO2- group in the ring and one or more double bonds in the ring are interrupted or the ring is optionally substituted by one or more CN, halo, OH, 1-6C alkyl, 3-6C cycloalkyl, 1-6C hydroxyalkyl, 1-6C alkoxyalkyl or NR3>R4> or -COR6> or (hetero)aryl, which is optionally with halo, 1-6C alkoxy, COR6> or (hetero)aryl; either R3>, R4>1-6C alkyl, 1-6C-alkoxy, -CO-1-6C alkyl (all optionally substituted with halo, OH, 3-6C heterocycloalkyl, 1-6C hydroxyalkoxy or NR3>R4>) or aryl and the heterocycloalkyl is optionally substituted by one or more N, O or S or -(CO)- or -SO2- group in the ring and one or more double bonds in the ring are interrupted or 3-6C heterocycloalkyl ring is optionally substituted by one or more CN, halo, OH, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C alkoxy, 3-6C cycloalkyl, -NR3>R4> or -CO-NR3>R4>, or H; or R3>R4>3-6C heterocycloalkyl ring interrupted by at least one nitrogen and optionally interrupted by one or more O or S, or -(CO)- or -SO2- group in the ring and one or more double bonds in the ring are interrupted or the ring is optionally substituted by one or more 1-6C alkyl, 3-6C cycloalkyl, 1-6C hydroxyalkyl, 1-6C alkoxyalkyl, CN, OH or NR3>R4>; R5>1-6C alkyl, 1-6C alkenyl, 1-6C alkynyl (all optionally substituted with halo, OH, CN, 1-6C alkoxy, 3-6C cycloalkyl, 3-6C heterocycloalkyl or NR3>R4>), where heterocycloalkyl is optionally interrupted by one or more N, O or S atoms or -(CO)- or -SO2- group in the ring and one or more double bonds in the ring are interrupted or the 3-6C heterocycloalkyl ring is optionally substituted by CN, halo, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C alkoxy, 3-6C cycloalkyl, NR3>R4>, -CO-NR3>R4>; R6>OH, 1-6C alkyl, 1-6C alkoxy or NR3>R4>; R7>-(CH2)n-aryl or -(CH2)n-heteroaryl; a
EP0987022B1 Conagenin for the treatment of ulcerous colitis and/or crohn's disease Preventives and remedies for ulcerous colitis and/or Crohn's disease containing as the active ingredient conagenin or a pharmaceutically acceptable salt thereof and having prominent therapeutic effects and a high safety.
WO2007071605A1 The use of st1898 for the treatment of restenosis The present invention relates to the use of a compound belonging to the class of atypical retinoids for the preparation of a medicament for treating pathological states, which arise from a complex series of cellular responses to vascular injury, for example after some surgery procedures, such as angioplasty, bypass grafting, endartherectomy and stent implantation.
WO2006086821A1 ANTISENS MODULATION OF INTEGRIN α4 EXPRESSION A method for the treatment and/or prophylaxis of an animal having a respiratory disease or condition associated with airway hyperresponsiveness, eosinophilia, neutrophilia, leukocytes or overproduction of mucus and/or with the expression of integrin α4 comprising administering to the animal a composition comprising from. 0.001 to 1000 µg per kg body weight of the animal of an antisense compound targeted to a nucleic acid molecule encoding integrin α4.
US20110301110 TRIM33 (TIF1gamma) AS A NEW DIAGNOSTIC MARKER OF CHRONIC MYELOMONOCYTIC LEUKEMIA (CMML) A method for diagnosing a chronic myelomonocytic leukemia (CMML) in a subject includes the steps of (i) determining the level of expression of the Trim33 (tripartite motif-containing 33) gene in a biological sample from the subject, and (ii) comparing the level of expression of the Trim33 gene in the biological sample with its normal level of expression; wherein an under-expression of the Trim33 gene is associated with CMML, and to a kit for diagnosing CMML in a subject including at least one nucleic acid probe or oligonucleotide or at least one antibody, which can be used in a such a method.
WO2012076832A1 Suppositories comprising rifaximin A pharmaceutical composition comprising rifaximin in the form of a suppository dosage form.
EP2495238A1 Novel 3-hydroxy-5-arylisoxazole derivative [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is a specific cyclic group; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is -CH2-, O, -S(O)i- (i is 0 to 2), or -NR7-; R1 to R6 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
WO2007113260A1 Azabicyclo [3. 1. o] hexyl derivatives as modulators of dopamine d3 receptors The present invention relates to novel compounds or pharmaceutically acceptable saltsthereof: wherein G is selected from a group consisting of : phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; A is a group P wherein P is p is an integer ranging from 0 to 5; Rl, R2, R3, R4,R5 and R7 are as defined in the claims, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
US20050020480 Administering a steroid The present invention relates to a method for the treatment of a patient suffering from major depressive disorder by administering to the patient an effective amount of a glucocorticoid receptor antagonist and to methods for establishing the optimal treatment regimen.
EP2550274A1 Pyrrolopyrazine derivatives and their use as jak and syk inhibitors The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables Q, R2, R3, and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
CN102552409A Compound orlistat nano-emulsion oral liquid and preparation method thereof The invention discloses a compound orlistat nano-emulsion oral liquid which contains the following components by mass percentage: 35%-45% of surfactant, 0-1% of cosurfactant, 0-1% of oil phase, 0.5%-4% of orlistat, 0.5%-3% of fructus cannabis oil, 0.5%-2% of evening primrose oil, 0.1%-0.5% of beta-carotene, 0.0001%-0.002% of vitamin D, 0.1%-0.5% of vitamin E, 0.0001-0.002% of vitamin K, and the balance of deionized water, and the sum of the mass percentage of the components is 100 percent. Aiming at the features of obese patients, the compound orlistat nano-emulsion oral liquid has multiple effects of reducing absorption of fat and heat in food, accelerating consumption of stubborn brown adipose tissues accumulated in the body, replenishing micronutrient matters lost during weight loss, reducing blood fat and cholesterol and the like, and does not have the side effects of insomnia, strength lack, palpitation and the like.
US20110294885 Controlled-release pregabalin compositions An orally-administrable controlled-release formulation, including pregabalin or a pharmaceutically acceptable salt of pregabalin and polycarbophil, as a controlled-release agent.
WO2013048177A3 Selenophene-fused aromatic compound and manufacturing method thereof Provided are a selenophene-fused aromatic compound, and a manufacturing method of the selenophene-fused aromatic compound.
CN103242407A Polyunsaturated fatty acyl group-containing phosphatidyl sterol and/or phosphatidyl stanol, and preparation method and application of same The invention provides phosphatidyl sterol and/or phosphatidyl stanol rich in polyunsaturated fatty acyl group, and a preparation method of the same, and mainly solves the technical problems that the existing phytosterol is poor in solubility and low in bioavailability, toxic agents are used in the preparation method of ester of the existing phytosterol, the reaction conditions are rigorous, and industrial production cannot be realized, and the like. The structural formula of phosphatidyl sterol and/or phosphatidyl stanol is shown in the specification, wherein Sn-1, Sn-2 and Sn-3 respectively refer to position 1, position 2 and position 3 of glyceride group in phospholipid; R1 and R2 are one of the following groups: -C19H29, -C19H31, -C21H31 or -C21H33, and X is sterol or stanol. The polyunsaturated fatty acyl group-containing phosphatidyl sterol and/or phosphatidyl stanol can effectively lower the effect value of cholesterol and triglyceride content in blood plasma; and application field and range of the polyunsaturated fatty acyl group-containing phosphatidyl sterol and/or phosphatidyl stanol are also provided.
US20100035994 Novel hydrate form of o-desmethyl venlafaxine succinate The present invention relates to a novel hydrate form of O-desmethyl venlafaxine succinate. The present invention further relates to processes for the preparation of the novel hydrate form, pharmaceutical compositions comprising it, second medical uses of the novel hydrate form, and methods using it for treating diseases such as generalised anxiety disorder, anxiety, depressive disorder, depression and panic disorder.
CN102532154A Angelica oncosepala linear furocoumarins compound and application thereof The invention relates to new compounds, in particular linear furanocoumarin compounds with antitumor activity and pharmaceutical application thereof. The general formula of an angelica oncosepala linear furocoumarins compound is shown in the description, wherein R is -H or -CH(CH3)2. The invention relates to the application of the angelica oncosepala linear furocoumarins compound in preparation of tumor cell inhibiting medicines.
CN101757640A Preparation of clathrate compound containing isoflavone and cyclodextrin of chickpea The invention relates to preparation of clathrate compound containing isoflavone and cyclodextrin of chickpea, comprising the following steps: grinding the chickpea into powder, drying, adding petroleum ether, backflowing for 1.5 hours in water bath with the temperature of 70 DEG C, filtering and drying; adding 65% alcohol, putting the obtained mixture in water bath with the temperature of 85 DEG C, backflowing for 1.5 hours, carrying out backflowing for two times, and filtering; adding distilled water, pouring the distilled water into a macroporous absorbing column, adjusting the flow rate to be 1ml/min, using a beaker to receive samples passing the column; adding 70% alcohol, adjusting the flow rate to be 0.5ml/min, collecting flow liquid, and distilling to obtain pure flavone; charging cyclodextrin and pure isoflavone with the mass ratio of 4-6:1, adding 2-4 times of water under normal temperature, grinding the mixture to be pasty, vacuum-drying, cleaning with alcohol, and drying to obtain the clathrate compound. The preparation has simple method, low cost, little toxicity of selected microcapsule wall materials, can increase the solubility of botanical drug after clathrate, improve the bioavailability of isoflavone and has good application prospect.
US20050043335 Heterocyclic derivatives of glycinamide and their medical use Compounds of the formula (I) are inhibitors of the enzyme Lp-PLA 2? and are of use in therapy, in particular for treating atherosclerosis.
CA2361496C Ph independent extended release pharmaceutical formulation Pharmaceutical formulations of acidic pharmacologic agents which demonstrate improved uniformity of release over the wide range of pH values encountered between the stomach and intestinal tract comprise an acidic pharmacologic agent dissolved or dispersed in a matrix comprising about 10 weight percent to about 40 weight percent of a neutral water-swellable hydrophilic polymer and 20 weight percent to about 50 weight percent of an acid-soluble polymer which swells in water at pH values above about 5. A particularly preferred formulation comprises divalproex sodium. Also disclosed are pre-tablet granulations and process for preparing both the pre-tablet granulation and the tablet unit dosage form.
US20050032758 Hormone replacement therapy and depression The treatment and/or prevention of depression by the co-administration of an estrogen with the progestin dienogest for HRT and/or contraception.
CN101879164A Frog-like cervical plexus block anesthetic substance The invention relates to the technical filed of medicine. In clinics at home and abroad, simple thyroid tumor surgeries mostly adopt cervical nerve block anesthesia, and the effect on researches of improving cervical nerve block anesthesia and reducing stress reaction during surgery is not ideal by using analgesics, beta-blocker and the like. The invention aims to provide a frog-like cervical plexus block anesthetic substance specifically applied to thyroid surgeries and the specific applicable concentration and dosage of the anesthetic substance which is 30ml of ropivacaine injection with the concentration of 0.25% (containing 75mg of ropivacaine), which can improve cervical nerve block anesthesia and reduce stress reaction during surgery. The invention has accurate positioning, simple operation, good block effect, few complications, high security and greatly reduced medical cost.
WO2007002441A1 Methods of use for non-atp competitive tyrosine kinase inhibitors to treat pathogenic infection Compositions and methods are provided for using non-ATP competitive tyrosine kinase inhibitors to treat pathogenic infection. In particular, methods for using non-ATP competitive inhibitors such as amino-substituted (E)-2,6-dialkoxystyryl 4-substituted- benzylsulfones, particularly ON012380, to treat pathogenic infection are provided. Infections to be treated according to the present invention include, particularly, those caused by microbial pathogens such as bacteria and viruses.
US6884799 Non-cross-linking pyrrolo[2,1-c][1,4]benzodiazepines and process thereof The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepines compounds of general formula V as shown below, which are useful as potential antitumour agents and a process of preparing these compounds; particularly the present invention provides a process for the preparation of 7-methoxy-8-{n-[7-methoxy-(11aS)-1,2,3,10,11,11a-hexahydro-5H-pyrrolo[2,1-c][1,4]ben-zodiazepine-5-one-8-yloxy]alkyloxy}-(11aS)-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one, with varying aliphatic chain length and its 2-hydroxy derivatives.
CN102824342A Compound used as antiepileptic medicine, and pharmaceutically acceptable salt thereof The invention relates to a compound represented by a general formula I, an addition salt thereof with a pharmaceutically acceptable acid, and an application of a medicine composition in preparing antiepileptic medicines.
WO2007054508A1 Pyrrolopyridines as kinase inhibitors The present invention is directed to compounds of the formula (I) or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disreguiated cell proliferation or to disregutated protein kinase.
CN101836964A Antibiotic and use method of control agent for controlling micro organism quantity The invention relates to antibiotic and use method of control agent for controlling quantity of fungus, bacterium, nematode, protozoa and other organisms which can cause poultry, pig, cattle, sheep and other animals to be ill. The method has obvious advantages compared with the conventional method: no investment is required on storage tank or preparation equipment, requirement for professional persons is reduced, work load is reduced, while efficiency of the applied medicine and nutrition component is better, the probability that the medicine and nutrition component are polluted after being diluted into solution is reduced, dosage is controlled to be in the required parameter range for specific animal feeding, degradation caused by light irradiation is eliminated, all the animals are ensured to accept the medicine in time period, food waste is reduced, and mixing and stirring are not required to be carried out on all the components when the components are added into the food for animals.
WO2006038719A1 Phosphonic acid derivative and therapeutic agent for disease in which high phosphate level in blood participates A novel compound represented by the following general formula (I), which has the function of reducing blood phosphate concentration. General formula (I): [In the formula, A represents -(CH2)n-, -CO-, -(CH2)n-CO-(CH2)m-, -(CH2)n-CS-(CH2)m-, or branched alkylene; rings B and C may be the same or different and each represents a benzene ring, naphthalene ring, azulene ring, heterocycle, or fused heterocycle; D represents -(CH2)(n+1)-, -(CH2)n-O-(CH2)m-, -(CH2)n-S(O)o-(CH2)m-, -CF2-, or -(CH2)n-NR10-(CH2)m- (provided that D is bonded to a carbon atom as a constituent member of the ring C); E represents oxygen or sulfur; P represents phosphorus; R1 to R7 may be the same or different and each represents a substituent (provided that R1 and R4 may be bonded respectively to R2 and R5 in cooperation with the adjacent carbon atom to form a 5- to 7-membered (un)saturated hydrocarbon ring or 5- or 6-membered fused heterocycle, and that when ring B is a benzene ring, not all of R1, R2, and R3 are hydrogen); and R8 and R9 may be the same or different and each represents a substituent; provided that R10 represents hydrogen, alkyl, etc., n and m each is an integer of 0-10, and o is an integer of 0-2.]
WO2009079401A2 Compositions and methods for increasing iron absorption Methods and compositions are provided for increasing iron absorption or in a human or animal. The methods and compositions provide iron and enzymatically hydroiyzed peptides.
CN101897671A Xylitol micro pill preparations and preparation method thereof The invention relates to xylitol micro pill preparations and a preparation method thereof. The preparations are the micro pills and comprise the following components in percentage by weight: 75 to 90 percent of xylitol, 1 to 10 percent of adhesive, 1 to 10 percent of coating substance, 1 to 5 percent of plasticizer, 0.5 to 2 percent of antisticking agent and a proper amount of solvent. In the xylitol micro pill preparations, the micro pills are prepared from the xylitol, so that the moisture absorption and deliquesce of the xylitol is effectively avoided, and meanwhile, when the micro pills are chewed, the micro pills can also be bit through, and the taste is not influenced; the micro pills have the effect of sustained release, so that the taking times are reduced, and compliance is intensified; the micro pills are not fractured, and the sweet taste is controlled, so that people who do not like the sweet taste can take the micro pills conveniently; and the stability of the prepared xylitol micro pills is high, and deterioration caused by the moisture absorption of the xylitol can be avoided.
CN103040987A Health protection preparation The invention relates to a health protection preparation, which is mainly composed of nutritional zinc and morinda officinalis. The product has the effects of invigorating the kidney, strengthening Yang and the like and can be prepared into forms of capsules, tablets, granules, oral liquid, powder and the like.
EP1744769A1 Non-staining topical iodine composition Non-staining topical iodine disinfecting compositions having the ability to inactivate pathogens associated with skin infections or diseases based upon the presence of molecular iodine in a concentration above at least 15 ppm. Any other iodine species selected from the group consisting of complexed iodine and triiodide may be present with the total of such other iodine species limited to a concentration of less than about 700 ppm so that any visible stain resulting from the application of this composition on the skin will dissipate without leaving any visible skin coloration.
US20110020426 Process for the continuous manufacture of a polyisobutylene based transdermal patch The present invention is directed to a process for manufacturing a transdermal delivery device comprising a backing layer, a release liner, and an adhesive layer between the backing layer and release liner. More specifically, the invention is directed to a process of preparing an adhesive layer, wherein the adhesive layer is comprised of polyisobutylene and an active pharmaceutical ingredient.
WO2012094293A1 Compositions comprising and methods of using inhibitors of sodium-glucose cotransporters 1 and 2 Pharmaceutical dosage forms useful for improving the cardiovascular and/or metabolic health of patients, particularly those suffering from type 2 diabetes, are disclosed, as well as methods of their manufacture.
US20080044486 Controlled Food Effect Composition The invention provides a pharmaceutical composition for oral administration comprising an active substance having a food effect, in combination with a lipid material comprising membrane lipids, which is characterised in showing a reduced food effect. The invention also refers to the use of a lipid material comprising membrane lipids for the manufacture of a pharmaceutical composition having a reduced food effect.
WO2014048065A1 Triazolyl derivatives as syk inhibitors Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
CN101006806A Mix oil containing linoleic acid and linolenic acid in the ratio of 4 to 1 The invention provides a kind of healthy harmonized oil containing linoleic acid and linolenic acid at a ratio of 4:1 for olders. The harmonized oil is composed of perillartine, oleum lini, sunflower oil, olive oil and bean oil at an uncertain ratio. There is 50wt.% essential fatty acid, 40wt.% linoleic acid, 10wt.% linolenic acid in the harmonized oil. Linolenic acid (C18:3, Omega-3) which can grow to eicosapentaenoic acid (EPA, C20:5, Omega-3) under the affect of enzyme of human liver is added into the edible vegetable oil. EPA is considered to be the main substance capable of cleaning blood dirties in blood vessels. EPA can also grow to docosahexaenoic acid (C22:6, Omega- 3) which is the core substance for forming brain and amphiblestroid membrane occupying one quarter of the whole brain and is called as brain gold by nutritionist. Thus, the prescription has influential contribution in preventing various kinds of angiocardiopathy and cerebrovascular disease, cleaning impurities in blood, slowing down the brain cell senescence, increasing intelligence, protecting eyesight, and suppressing anaphylactic response.
WO2012170384A1 Use of metallocene compounds for cancer treatment Metallocene compounds and pharmaceutical compositions containing these metallocene compounds are disclosed and described. Methods of treating cancer employing such metallocene compounds and pharmaceutical compositions also are provided.
WO2006092822A2 4-fluorophenyl-derivatives of 1-{[1,5 -bis (4-chloro phenyl) -2-methyl-1h-pyrrol-3-yl]methyl} -4- methylpi pεrazine, synthesis process and uses thereof The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4- chlorophenyl)-2-methyl-lH-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds.
US8268894 Compositions and methods for the treatment of infectious diseases Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
US20120245201 Isopropylphenidate for Treatment of Attention-Deficit/Hyperactivity Disorder and Fatigue-Related Disorders and Conditions The present invention relates to the identification of isopropylphenidate as a useful therapeutic agent in the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) as well as various fatigue causing disease and disorders and medication induced fatigue.
EP0925356B1 New antigen presenting cells, a process for preparing the same and their use as cellular vaccines The invention relates to monocytes derived antigen presenting cells (MD-APCs) characterized in that they have the following properties: they present on their surface: antigen CD14 and CD64 with a mean intensity of about 5 to about 200; antigen CD80 and CD86 with a mean intensity of about 20 to about 200; antigen CD40 and mannose receptor with a mean intensity of 50 to 500; they are substantially devoid of the surface antigens CD1a and CD1c; they present a phagocytosis property; they have the property of stimulating the proliferation of allogenic lymphocytes.
WO2011074608A1 Prophylactic or therapeutic agent for chronic hepatitis c Disclosed is a prophylactic or therapeutic agent for chronic hepatitis C, which contains a triterpene derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. (In formula (I), R1 represents a hydrogen atom or a hydroxyl group; R2 represents a C1-6 alkyl group, -CH2OR7 or -CON(R8)R9; R3 and R4 may be the same or different and each represents a hydrogen atom, a hydroxyl group or the like; and R5 and R6 may be the same or different and each represents a hydrogen atom, a hydroxyl group or an alkoxy group. In this connection, R7 represents a hydrogen atom, a C1-6 alkyl group or the like; and R8 and R9 may be the same or different and each represents a hydrogen atom, a C1-6 alkyl group or the like. Also in formula (I), the broken line (-----) represents a single bond or a double bond, and when the broken line represents a double bond, R4 and R6 are not in existence. In this regard, 22β-methoxyolean-12-ene-3β,24-diol is excluded from the triterpene derivatives represented by formula (I).)
EP2755662A1 Combination therapy using ribavirin as eif4e inhibitor The present invention relates to pharmaceutical compositions and combination therapies for treating patents having a neoplasm or proliferative disorder, the combination comprises an inhibitor of the elF4E gene product and a chemotherapeutic agent, wherein said combination therapy overcomes resistance developed in patients during anti-neoplastic treatment. The present invention also provides for the use of a combination therapy for treating patients having a neoplasm, a proliferative disorder, pre-neoplasm or a precancerous lesion, comprising an inhibitor of the elF4E gene product, a chemotherapeutic agent, and a therapeutically effective amount of a hedgehog pathway inhibitor, and the method of using said combination therapy.
EP1774974A1 Use of hyperforin or St. John's Wort in the treatment and prevention of metabolic syndrome The invention relates to the use of hyperforin, its derivatives or a hyperforin-containing extract of Hypericum perforatum L. (St. John's Wort) for the manufacture of a pharamaceutical composition for the treatment or prevention of Metabolic Syndrome and to a method of treating or preventing Metabolic Syndrome by administering to a patient in need of such treatment an effective amount of hyperforin, its derivatives or a hyperforin-containing extract of Hypericum perforatum L (St. John's Wort).
CN102198176A Formula for main product mainly comprising rosemary The invention relates to an external use medicine for invigorating blood, eliminating swelling, reliving pain and preventing insect bites, which takes rosemary, monkshood, radix aconiti agrestis, notopterygium roots, radix angelicae pubescentis, ligusticum wallichii, angelica, anise, cumin, angelica roots, cinnamon, papaya, common peony roots, and safflowers as raw materials. The above raw materials are prepared into an external use medicament through a permeability processing technique. The medicament has functions of relaxing tendons, activating collaterals, invigorating blood, reliving pain, and eliminating swelling and blood stasis, is suitable for treating trauma caused by falling, striking, twisting, and pulling. The invention has advantages of convenience in use and no toxic and side effects, and is especially suitable for travel enthusiasts to carry during travel.
US20090082419 Deuterium-enriched tegaserod The present application describes deuterium-enriched tegaserod, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US7825216 Phenylanine derivatives The present invention provides phenylalanine derivatives that inhibit SH2 domain binding with a phosphoprotein. These derivatives include compounds of the formula: W—Y-(AA)n-Z wherein n is 0 to 15; Y is a phenylalanyl radical having a phenyl ring, an amine end, and a carboxyl end, the phenyl ring having one or more substituents, e.g., hydroxyl, carboxyl, formyl, carboxyalkyl, carboxyalkyloxy, dicarboxyalkyl, dicarboxyalkyloxy, dicarboxyhaloalkyl, dicarboxyhaloalkyloxy, and phosphonoalkyl, or phosphonohaloalkyl; W is a moiety attached to the nitrogen of Y and is, e.g., alkylcarbonyl, oxalyl, alkylaminooxalyl, arylaminooxalyl, arylalkylaminooxalyl, or alkoxyoxalyl; AA is an amino acid, the amine end of which is attached to the carboxyl end of Y; and Z is an arylalkylamino or arylheterocyclyl alkylamino; or a salt thereof; with the proviso that W is not arylalkylamino when the phenyl ring of phenylalanyl contains a phosphonoalkyl or phosphonohaloalkyl substituent at a position para to the alkylamido group and the ortho and meta positions are unsubstituted. The present invention further provides precursors suitable for preparing the phenylalanine derivatives and a method for the preparation of the precursors. The present invention further provides conjugates comprising a precursor and a conjugant that are covalently linked. These conjugates have biological and/or pharmacological properties.
CN102614309A Cataplasm for treating body surface skin ulcer The invention discloses cataplasm for treating body surface skin ulcer, which is applied to the technical field of medicine. The formula of a product comprises cinnabar, roasted calamine, French chalk, borneol, sheet chestnut powder, peach gum, ethylene diamine tetraacetic acid disodium salt, sodium polyacrylate, polyvinylpyrrolidone, sodium carboxymethylcellulose, kaolin, glycerol, dihydroxyaluminium aminoacetate, tartaric acid, azone and water. A preparation method of the cataplasm comprises the following steps of: fully dissolving polyvinylpyrrolidone into water, adding sodium carboxymethylcellulose and peach gum, and continually adding tartaric acid to obtain a mixed solution 1 (water phase); putting the sodium polyacrylate, ethylene diamine tetraacetic acid disodium salt, dihydroxyaluminium aminoacetate, azone and kaolin into glycerol, stirring to fully expand, and adding cinnabar, roasted calamine, French chalk, sheet chestnut powder, borneol ultrafine powder to obtain a mixed solution 2 (oil phase); and adding the water phase into the oil phase, coating paste on a medical non-woven fabric in a hot state by using a flattening method, pasting a film, slicing, standing and fully crosslinking to obtain cataplasm. The cataplasm has the advantages of simple use method, no influence on the stability of a main medicament, no side effect, no skin excitation or sensitive reaction, and no residue on skin.
CN103183675A Phosphodiesterase-4 inhibitor The invention belongs to the technical field of medicines and particularly relates to a phosphodiesterase-4 inhibitor as shown in a general formula (I) and a pharmaceutically acceptable salt, a stereoisomer or a solvent compound thereof. In the formula, R1, R2, R3, R4, R5, R6, R7, R8, R9, R7', R8', R9', L and a ring A are as defined in the specification. The invention further relates to a preparation method for the compound, a pharmaceutical composition with the compound, and an application of the compound and the pharmaceutical composition to preparation of drugs for treating and/or preventing inflammatory diseases, disease symptoms and disease conditions characterized by or related with undesired inflammatory immune reaction and all diseases induced by or related with TNF-alpha (tumor necrosis factor-alpha) and PDE-4 (phosphodiesterase-4) hypersecretion.
WO2013100822A3 Hemostimulating agent The present invention proposes a combination of a bis-(γ-L-glutamyl)-L-cysteinyl-glycine dilithium salt and coordination compounds formed by palladium, copper and (γ-L-glutamyl)-L-cysteinyl-glycine, a pharmaceutical composition containing said combination, and a method for stimulating hemopoiesis using same.
WO2004096823A3 Novel ketolide derivatives Antimierobial ketolide compounds are provided having the formula (A), as well as pharmaceutically acceptable salts, esters or prodrugs thereof, pharmaceutical compositions comprising such compounds, methods of treating bacterial infections by the administration of such compounds, and processes for the preparation of the compounds.
WO2003098385A3 System and method for transparent early detection, warning, and intervention during a medical procedure The present invention relates, in general, to prevention of false, annoying, or oversensitive alarms, providing early detection by a sensitive test, generating silent, semi-overt, or overt alarm conditions and/or initiating early passive or active interventions to untoward events. The invention buys time by providing an early intervention in the event that a highly sensitive early detection is later confirmed by a specific test. A particular embodiment of the invention is directed to the early detection of hypoventilation, including apnea and airway obstruction, and the pausing or interrupting of an auction such as drug delivery during medical procedures.
US7981448 Method of treating necrotizing enterocolitis in a patient, which includes administering a pharmaceutical composition that includes carbon monoxide to the patient. The present invention relates to a method of treating necrotizing enterocolitis in a patient, which includes administering a pharmaceutical composition that includes carbon monoxide to the patient.
WO2011067653A1 Oral compositions for use in the mercury intoxication from dental amalgam The invention refers to a composition to treat or prevent in subjects with sub-clinical or acute mercury intoxication from dental amalgam, or a diagnostic tool thereof. The odontostamatologic composition comprising at least a non-resorbable, preoxidised or fully oxidised thiolated polymer are used as efficient detoxifying products in oral care; or as diagnostic aid to asses the mercury exposure on mouth in subjects with dental amalgam. Inventive compositions include dentifrices, pastes, gel, mouthwashes, dental trays, and protective mask for dentistry professionals comprising thiolated polymers such as partially or fully oxidised micronized macroporous or hydrocolloidal thiolated polymers, or urea- functionalized polymer affording the broad sequestration of the intra-oral mercury.
WO2010078294A1 Method of preparing (+)-1,4-dihydro-7-[(3s,4s)-3methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid Methods of preparing (+)-1, 4-dihydro-7-[(3S,45)-3-methoxy-4-(methylamino)-1 - pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.
CN103462972A Application of Incarviatone A in anti-lung cancer metastasis medicaments The invention discloses an application of Incarviatone A in preparation of anti-lung cancer metastasis medicaments, and belongs to the technical field of a new application of medicaments. The Incarviatone A can inhibit the movement and migration capability of tumor cells. The application of the Incarviatone A in preparation of the anti-lung cancer metastasis medicaments is made public for the first time, the skeleton type is completely novel, and the Incarviatone A has an unexpectedly strong metastasis inhibiting activity of lung cancer cells.
WO2006134828A1 Anion adsorbent, agent for purifying water or soil, and method for producing those Disclosed is a novel anion adsorbent having extremely high anion adsorbing ability. This anion adsorbent is mainly composed of iron as a metal that is excellent in biological safety. Specifically disclosed is an anion adsorbent containing, as an active ingredient, an amorphous ferric hydroxide which is produced in the presence of a ferrous species.
EP2298762A2 Heterobicyclic compounds with antibacterial activity Naphthalene derivatives (or mono- or polyaza analogs) (I), having a side-chain containing a cycloalkylene, heterocycloalkylene, arylene or heteroarylene group in the 1-position, are new. Naphthalene or mono- or polyaza-naphthalene derivatives of formula (I) and their salts, solvates and hydrates are new; [Image] A : O, S, NH, alkylene, alkenylene, alkynylene or heteroalkylene; X 1>-X 5>N, CH or CR 4>; Cy : cycloalkylene, heterocycloalkylene, arylene or heteroarylene; R 1>H, halo, OH, NH 2, SH, alkyl, heteroalkyl, alkoxy, heteroalkoxy, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, cycloalkoxy, alkylcycloalkoxy, heterocycloalkoxy or heteroalkylcycloalkoxy; R 2>halo, OH, NH 2, SH, alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl; or two R 2> groups together form part of an aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, aralkyl or heteroaralkyl ring; R 3>alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl; R 4>halo, OH, alkyl, alkenyl, alkynyl or heteroaralkyl; and m, n : 0-2. - ACTIVITY : Antibacterial. - MECHANISM OF ACTION : DNA Gyrase Inhibitor; Topoisomerase IV Inhibitor.
WO2011076854A1 CLEAVAGE OF β-AMYLOID PRECURSOR PROTEIN The present invention concerns methods and means for the identification of meprin-α and meprin-β as novel β-secretases and antagonists thereof for use in the treatment of amyloidosis.
WO2013020302A1 Diclofenac sodium sustained release tablet and preparation process therefor A diclofenac sodium sustained release tablet and a preparation process therefor. The diclofenac sodium sustained release tablet comprises the following components: diclofenac sodium 16.5-39.0%, a sustained-release agent 10.0-35.5%, a filler 33.5-65.0%, a glidant 2.01-8.0%, a lubricant 0-2.5%, and a binder 0-8.0%. The diclofenac sodium sustained release tablet is prepared by a full-powder direct tabletting process, which prevents coagulation of particles, and at the same time does not use high-concentration alcohol.
CN1771956A Itraconazole dripping pill and its prepn The present invention discloses one kind of orally taken antifungal medicine composition, and aims at providing one kind of antifungal itraconazole dripping pill with high bioavailability, fast medicine release, fast acting, high medicine content, easy taking, low cost and production process without pollution. The itraconazole dripping pill is prepared with itraconazole as medicine material and medicine carrier as matrix.
WO2013034863A1 Scheme for administering n-hydroxy-4-{2-[3-(n,n-dimethylaminomethyl)benzofuran-2-ylcarbonylamino]ethoxy}benzamide A novel scheme for administering N-hydroxy-4-{2-[3-{N,N-dimethylaminomethyl)benzofuran-2-ylcarbonylamino]ethoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, alone or in combination with a surgical, chemotherapy or hormone therapy treatment or with radiotherapy, for the treatment of cancer, characterized in that it is administered for 4 consecutive days, this period being followed by 3 consecutive days without any administration of the compound of formula (I), wherein it is understood that the chemotherapy treatment is not FOLFOX.
CN101347409A Sustained-release injection containing octadecyl dimethyl-4-piperidine phosphate A sustained release anti-cancer injection with edelfosine consists of the edelfosine with effective anti-cancer amount and an amphiphilic block copolymer hydrogel, wherein, part or the whole of the edelfosine is encapsulated in sustained release microsphere and exists singly in the form of the sustained release microsphere or microsphere and micro-powder in the sustained release injection. The amphiphilic block copolymer hydrogel is selected from PLGA-polyethylene glycol-PLGA, sustained release gel has temperature-sensitive gelation property; and the sustained release gel is flowable fluid in an environment below body temperature, and can automatically change into biodegradable and absorbable non-flowable water-insoluble gel in bodies of warm blooded animals, thus causing the drug to be slowly released in the local part of tumor; the sustained release microsphere is favorable to the stable and sustained release of the drug, the dual sustained release is beneficial to controlling tumor cells in dormancy stage, the drug in the form of the micro-powder in the sustained release gel is favorable to the relatively quick release, thus being beneficial to controlling cells with quicker proliferation. The sustained release anti-cancer injection with edelfosine can be used together with radiotherapeutic particles, chemotherapeutic drugs, etc.
WO2013006758A1 Diphosphate mimetics and uses thereof The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N- acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLKl inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and/or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and/or kinase-associated conditions.
WO2010037892A1 Composition comprising silibinin at determined concentrations and combined preparation comprising silibinin and a pi3k/akt pathway inhibitor for the treatment of cancer The present invention relates to the use of a composition comprising silibinin in the required proportion to attain concentrations in serum equal to or exceeding 250 μM, or alternatively silibilin and an Akt inhibitor, for the preparation of a medicament for the treatment of cancer, and a combined preparation of, at least, silibinin and an inhibitor of the PI3K/Akt pathway, for the separate, simultaneous or sequential use thereof in the treatment of cancer.
CN103599537A Pharmaceutical composition of calcium channel blocker/thiazide diuretic/5-methyltetrahydrofolate The invention relates to a pharmaceutical composition containing a calcium channel blocker (CCB), thiazide diuretic and 5-methyltetrahydrofolate, and use of the pharmaceutical composition. The pharmaceutical composition comprises medicinal dose of CCB, medicinal dose of thiazide diuretic, medicinal dose of 5-methyltetrahydrofolate and a pharmaceutically-acceptable carrier. The invention provides use of the pharmaceutical composition in preparation of a medicament for treating hypertension, and preventing, treating or delaying a target-organ damage caused by the hypertension. The invention also provides use of the pharmaceutical composition in preparation of a medicament for reducing the dangerousness of cardiovascular and cerebrovascular events caused by the hypertension. By implementation of the pharmaceutical composition, the pharmaceutical composition with specific use is supplied to a sufferer; the medication compliance of the sufferer also can be increased; the curative effect also can be improved.
EP2605762A1 Compositions comprising adipose tissue and a pge2 analogue and their use in the treatment of a soft tissue condition The present invention is directed to compositions and methods of transplanting tissue, for example, in breast augmentation procedures. The compositions include adipose tissue and compounds that reduce tissue volume loss and increase survival rate of the adipose tissue when the composition is introduced into breast tissue.
CN1927342A Heat clearing and detoxicating dispersant tablet and method for making same The invention relates to dispersible tablets for heat clearing and detoxicating, as well as the preparing process, wherein the raw materials include gypsum, scrophularia root, dried rehmannia root, capsule of weeping forsythia, cape jasmine, Herba Corydalis bungeanae, rough gentian, isatic root, anemarrhena rhizome, lilyturf root, honeysuckle flower, and baikal skullcap root.
US8802636 Combination therapy for treatment of sleep apnea The present invention features a novel therapy for effecting weight loss which involves treating a subject with a sympathomimetic agent (e.g., phentermine or a phentermine-like drug) in combination with an anticonvulsant sulfamate derivative (e.g., topiramate) such that the subject experiences weight loss. The combination methods of the present invention also are effective against symptoms associated with Syndrome X. The invention also features pharmaceutical compositions and kits for use in the practice of these novel therapies.
CN102558222A Resveratrol germanium sesquioxide compound, preparation method thereof and application thereof The invention discloses a resveratrol germanium sesquioxide compound, a preparation method thereof and application thereof. The method for preparing the resveratrol germanium sesquioxide compound comprises the following steps of: performing addition reaction of double bonds in a raw material with a resveratrol structure by germanium chloroformer, and hydrolyzing the product which is subjected to addition to obtain the resveratrol germanium sesquioxide compound, wherein the raw material with the resveratrol structure is resveratrol or derivatives thereof. The resveratrol germanium sesquioxide compound has a Ge-O bond with high activity, so that the activity of the resveratrol is improved; and experiments prove that the resveratrol germanium sesquioxide compound has the activity which is higher than that of the resveratrol, and has a bright application prospect in the preparation of antioxidative, anti-tumor and anti-bacterial or immunoregulatory medicines.
WO2011127519A1 Combination treatment with vegf-c antagonists The invention relates to a method and kit for treating cancer in a human subject, the method comprising administering to the subject in combination therapeutically effective amounts of a VEGF-C antagonist and an anti-neoplastic composition, and the kit comprising a VEGF-C antagonist for administering to the subject in combination with an anti-neoplastic composition. The invention further relates to methods for: increasing the duration of survival of, increasing the progression-free survival of, increasing the duration of response of, or treating, a subject or a group of human subjects susceptible to or diagnosed as having a cancer; or treating a human subject or a group of human subjects having metastatic colorectal cancer, prostate cancer, pancreatic cancer or glioblastoma, the methods comprising administering to the subject or subjects in the group in combination effective amounts of a VEGF-C antagonist and an anti-neoplastic composition.
WO2008103615A1 Isoquinolines useful as inducible nitric oxide synthase inhibitors Disclosed herein are new isoquinoline compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of nitric oxide synthase activity in a human or animal subject are also provided for the treatment disease.
US7393860 for the treatment of peptic ulcer disorders; (7R,8R,9R)-2,3-Dimethyl-8-hydroxy-7-(2-methoxyethoxy)-9-phenyl-7,8,9,10-tetrahydro-imidazo-[1,2-h][1,7] naphthyridine or a pharmaceutically acceptable salt The compound (7R,8R,9R)-2,3-Dimethyl-8-hydroxy-7-(2-methoxyethoxy)-9-phenyl-7,8,9,10-tetrahydro-imidazo-[1,2-h] [1,7] naphthyridine inhibits the secretion of gastric acid.
CN103387567A NEPT compound and preparation method and application thereof The invention discloses a NEPT compound and a preparation method and the application thereof. The NEPT compound is shown as formula I. This preparation method of the NEPT compound shown as the formula I comprises the following steps: (1) a compound shown as formula II reacts with ethylenediamine to obtain a compound shown as formula III; (2) a compound shown as formula IV reacts with 9-fluorene methyl-N-succinimido carbonate under alkaline conditions to obtain a compound shown as formula V; (3) the compound shown as the formula III reacts with the compound shown as the formula V in the presence of a condensing agent to obtain a compound shown as formula VI; (4) a deprotection reaction of the compound shown as the formula VI is carried out in the presence of an organic alkali to obtain a compound shown as formula VII; and (5) the compound shown as the formula VII reacts with a compound shown as formula VIII in the presence of the condensing agent to obtain the compound shown as the formula I; wherein, X is C, a first chemical group or a second chemical group (the first chemical group and the second chemical group are shown in the specification), and a compound shown as the formula I in which the X is NH is obtained by deprotection of the compound shown in the formula I in which the X is the second chemical group under acidic conditions. The invention also provides the application of the compound shown in the formula I in preparation of drugs for prevention and/or treatment of tumour.
CN101766566A Method for preparing injection of sodium ferulate The invention discloses a method for preparing an injection of sodium ferulate, belongs to the field of industrialized production of medicaments and relates to an injection of sodium ferulate. The method is characterized in that: the injection contains sodium ferulate, propylene glycol, amino acid and derivatives thereof and sodium metabisulfite. The invention discloses a method for preparing the injection of sodium ferulate, which is characterized in that the injection contains sodium ferulate, propylene glycol, methionine and sodium metabisulfite in a weight ratio of 1.0:0.05-5.0:0.01-5.0:0.01-1.0.
US20050107449 Substituted thiazoles and oxazoles, e.g., 4-{1-[4-[2-(2-Chloro-6-fluoro-phenyl)-ethyl]-2-(4-trifluoromethyl-phenyl)-thiazol-5-yl]-ethylsulfanyl}-2-methyl-phenoxy)-acetic acid; treating atherosclerosis and diabetes and creating Syndrome X The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I. (Formula I); wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, aryl (C0-C4) alkyl, aryloxy (C0-C4) alkyl, arylthio (C0-C4) alkyl, and further wherein when R5 is alkyl, R5 can optionally combine with W to form a 6 membered cycloheteroalkyl ring that is fused with the oxazole or thiazole ring to which the R5 group is attached; (b) R9 is selected from the group consisting of C1-C5 alkyl, C1-C5 alkenyl, and arylC0-C3alkyl. (c) T1 is selected from the group consisting of C and N, (d) W is selected from the group consisting of CH2, C(O)N(R21), N(R21), N(R21)CH2, O, OCH2, S, and SO2; and (e) X is selected from the group consisting of C, CH2C, and CCH2
CN103319427A Hexahydrobenzisoxazole compounds and application thereof The invention provides hexahydrobenzisoxazole compounds and an application thereof. The compounds are characterized in that the structural formula of the compounds is shown in the specification; and in the formula, each of R1, R2 and R4 is a methyl group, R3 is a hydroxy goup, and R5 is a phenyl group, a p-chlorophenyl group or a p-methylphenyl group. The novel hexahydrobenzisoxazole compounds are prepared through utilizing natural renewable resources in the invention. The invention also provides a synthesis method of the hexahydrobenzisoxazole compounds and an application of the hexahydrobenzisoxazole compounds in the activation of a PPAR-gamma channel. The method comprises the following steps: carrying out a condensation reaction of 2-hydroxy-2,6,6-trimethylbicyclo[3,1,1]heptyl-3-one and aromatic aldehyde to generate 4-arylmethylene-2-hydroxy-2,6,6-trimethylbicyclo[3,1,1]heptyl-3-one, and cyclizing 4-arylmethylene-2-hydroxy-2,6,6-trimethylbicyclo[3,1,1]heptyl-3-one and hydroxylamine hydrochloride to obtain the hexahydrobenzisoxazole compounds.
CA2468833C (20s)-1.alpha.-hydroxy-2-methylene-19-nor-bishomopregnacalciferol and its uses This invention discloses (20S)-1.alpha.-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, pharmaceutical uses therefor, and a method of purifying this compound to obtain it in crystalline form. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat immune disorders in humans as well as renal osteodystrophy.
WO2013054267A1 Synergistic composition for preventing and treating disorders connected with ageing Pharmaceutical or dietary supplement composition, comprising, as active ingredients with combined or synergistic effect, curcumin and astaxanthin, for use in the prevention and treatment of disorders connected with ageing of the organism.
EP2588453A1 Compositions and methods for modulating the wnt signaling pathway The present invention relates to compositions and methods for modulating the Wnt signaling pathway, using compounds having Formula (1) and (3): wherein A, B, Y and Z all represent rings, and R1, R2, R3 are as defined herein.
CN101926833A Hydrogel patch and preparation method thereof The invention relates to a hydrogel patch and a preparation method thereof. The hydrogel patch consists of three parts: bidirectional flexible non-woven fabric, medicament-containing paste and a cover film layer, wherein the main part, namely the medicament-containing paste is prepared from fluid extract and proper hydrogel matrixes such as an adhesive, a humectant, an excipient, a pH modifying agent, a cross-linking agent, a transdermal enhancer, a filler, a dispersant, a chelating agent, a tackifier and deionized water according to a proportion, wherein the tackifier is at least one of polyvinyl alcohol, povidone, gelatin, carboxymethyl cellulose, collagen, modified starch and plant polysaccharide, or is emulsion formed by polymerizing free radicals of 0-30 percent acrylic acid, 0 to 50 percent vinyl pyrrolidone and 0 to 50 percent 2-acrylamido-2-methylpropanesulfonic acid, and is added in an amount which is 5 to 15 percent based on the total weight. The hydrogel patch solves the common problem of poor viscosity of common hydrogel, and has the characteristics of high adhesion, high compliance with skin, quick response, reusability, moisture retention, permeability and comfortable use.
WO2005016325A2 CRISTALLINE ZIPRASIDONE HCl AND PROCESSES FOR PREPARATION THEREOF Provided is cristalline ziprasidone HCl and processes for preparation thereof.
EP1684768A2 Methods of treating eczema A method of treating eczema in a human or other mammal in need thereof comprising administering systemically to said human or other mammal a tetracycline compound in an amount that is effective to treat eczema, but has substantially no antibacterial activity.
US20080004281 Methods for the modulation of crp by the selective modulation of ppar delta The present invention discloses methods to reduce C-reactive protein (CRP) in patients in need thereof comprising the selective modulation of PPARδ.
CN1810239A Liver cancer cell inhibitor The present invention provides one kind of liver cancer cell inhibitor containing sesamin and relates to the use of sesamin in preparing liver cancer inhibitor. Specifically, the present invention provides the mechanism of sesamin in activating the cancer inhibiting gene p53 to inhibit the proliferation of liver cancer cell.
US7285642 Composition and method for modulating dendritic cell-T cell interaction The present invention relates to the use of a compound that binds to a C-type lectin on the surface of a dendritic cell, in the preparation of a composition for modulating, in particular reducing, the immune response in an animal, in particular a human or another mammal. The composition in particular modulates the interactions between a dendritic cell and a T-cell, more specifically between a C-type lectin on the surface of a dendritic cell and an ICAM receptor on the surface of a T-cell. The compositions can be used for preventing/inhibiting immune responses to specific antigens, for inducing tolerance, for immunotherapy, for immunosuppression, for the treatment of autoimmune diseases, and the treatment of allergy. The compound that binds to a C-type lectin is preferably chosen from mannose, fucose, plant lectins, antibiotics, sugars, proteins or antibodies against C-type lectins. The invention also relates to such antibodies.
US20110082091 Method for Preclinical Testing of Immunomodulatory Drugs The invention teaches a method for testing a prospective or known immunomodulatory drug for T-cell activation, comprising the step of contacting in-vitro a peripheral blood mononuclear cell (PBMC) culture with a predetermined amount of the prospective or known immunomodulatory drug and observing the PBMC culture for T-cell activation using a readout system, upon contact with the prospective or known immunomodulatory drug, wherein the cell density of a PBMC preculture is adjusted such that cell-cell contact of the PBMC is enabled and wherein the PBMC preculture is cultured for at least 12 h.
CN101245112B Polyoses extracted from pistacia chinensis meal and extracting method thereof The invention discloses a polysaccharide which is extracted from Chinese pistache and the extraction method; the polysaccharide is extracted by the following steps: the Chinese pistache raw material is added in the strong acidic solution, which is taken as extracting solution and has a concentration of 0.01 to 7mol/L, or the weak acid with the weight percentage concentration of 0.01 percent to 100 percent or the alkaline solution with the concentration of 0.05 to 8.0mol/L or the water according to the material liquid ratio of 1: 1 to 1:200g/ml and is taken out after 1 minute to 8 hours of extraction, the solution after removing the sediment is obtained by centrifugal separation or filtration, then the sufficient amount of solvent is added for full precipitation of the polysaccharide, finally the solution is removed by centrifugalization or filtration, anhydrous ethanol, propyl alcohol or propyl alcohol are used for washing for a plurality of times, and the crude polysaccharide is obtained by freeze drying. The extraction method takes the commonly used acidic solution and alkaline solution or water as the extracting liquid, the extraction conditions are simple and convenient, and the extraction method further takes the ultrasonic or microwave extraction as auxiliary means; the extraction method has higher polysaccharide yield, can greatly improve the additional values of processing and utilizing of the Chinese pistache and has great popularization and application prospects on the industrial aspect.
WO2007144503A3 Novel process for preparing nitrones and n-hydroxylamines comprising at least one hydroxyl group, and products thus obtained The present invention relates to the use of a Lewis acid, in particular chosen from: - boron trihalides (BI3, BBr3, BCl3, BF3), - complexes of the abovementioned boron trihalides with Lewis bases such as ethers, thioethers, phosphines or amines, or - trialkylsilane halides (TMSI, TMSBr), for converting one or more alkoxyl groups to one or more hydroxyl groups, wherein said alkoxyl groups are present on cyclic or noncyclic compounds bearing a nitrone or N-hydroxylamine nitrogenous functional group, it being possible for said nitrogenous functional group to be integrated into a ring, without affecting the nitrogenous functional group.
WO2007125731A1 Soft contact lens solution, drug-sustained release soft contact lens prepared by using the solution Disclosed is a soft contact lens solution which can alleviate an allergic condition without the need of administering a medicinal agent frequently in the form of an eye drop. Also disclosed is a method for production of the solution. A soft contact lens is contacted with a soft contact lens solution comprising an aqueous medium and polyphenol as an allergen-deactivating component contained in the aqueous medium, so that the allergen-deactivating component can be incorporated into the soft contact lens.
CN103450278A Water-soluble carbon monoxide releasing molecule and preparation method and application thereof The invention discloses a water-soluble carbon monoxide releasing molecule. The structural formula of the water-soluble carbon monoxide releasing molecule is shown in the following formulaspecification, wherein M is Cr or Mo; R1, R2, R3, R4 are independently benzyl or C1-C18 alkyls, any of R1, R2, R3, and R4 is benzyl, and the rest three are independently C1-C18 alkyls; and R5 is C1-C4 alkyls or phenyls. The compound has excellent controllable carbon monoxide slow release performance, water solubility and biocompatibility and excellent antimicrobial activity, and; as as shown in experimental results, the compound expresses broad-spectrum bactericidal performance to gram-positive bacterium and gram-negative bacterium, solves the problems of water solubility and CO slow release of the existing metal carbonyl carbon monoxide releasing molecule, overcomes the limitation of single antimicrobial target of the traditional antibiotics resulting in difficulty to effectively kill a variety of bacteria, and has a broad application prospect in the antimicrobial field.
EP1750664A1 Intravitreal implants in conjunction with photodynamic therapy to improve vision A method for treating a posterior ocular condition so as to improve vision is provided. The method includes the steps of placing into an eye, a bioerodible implant comprising an anti-inflammatory component and a bioerodible polymeric component, introducing a photoactive agent into the eye, and irradiating the eye with electromagnetic radiation, for example light energy, in order to activate the photoactive agent in the eye and treat the posterior ocular condition, thereby improving a patient’s vision.
WO2010147666A1 Compounds useful as carbonic anhydrase modulators and uses thereof Compounds are disclosed that have formula (I'): wherein A, W, Cy1, Cy2, L1, L2, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions thereof are useful as probes and imaging agents for identifying hypoxic tumors, and treatment of a variety of conditions such as cancers involving hypoxic tumors, in mammals including humans, including by way of non-limiting example, and others.
WO2012113963A1 Use of p53 inhibitors for reducing food intake and lowering body weight The present invention relates to the use of p53 inhibitors in the hypothalamus to reduce food intake and to lower body weight in the treatment of obesity or obesity-associated metabolic disorders.
CN101336893A Sustained-released injection containing bortezomib and topology enzyme inhibitor The invention relates to a slow-release injection containing bortezomib and topoismerase inhibitors. The slow-release injection is composed of slow-release microspheres and a solvent, wherein the slow-release microsphere contains an anticancer effective component selected from bortezomib and topoismerase inhibitor and a slow-release adjuvant, and the solvent is a common solvent or a special solvent containing suspending agent. The viscosity of the suspending agent is in the range from 100cp to 3000cp at a temperature ranging from 20 DEG C to 30 DEG C. The suspending agent is preferably sodium carboxymethylcellulose. The slow-release adjuvant is selected from a copolymer of poly(phosphate ester) (such as p(LAEG-EOP) and p(DAPG-EOP)) or a copolymer or a blend of poly(phosphate ester) and PLA or polifeprosan or PLGA or poly(erucic acid dipolymer-sebacic acid). The topoismerase inhibitor is selected from camptothecin, hydroxycamptothecine, topoteean, lurtotecan, irinotecan, etoposide and teniposide. The anticancer composition is also formulated as slow-release implant. After the intratumoral or peritumoral injection or implantation, the effective blood concentration lasts more than 60 days. Additionally, the slow-release injection can significantly reduce the general drug reaction and selectively enhance the chemotherapeutic effect, particularly the effect of non-operative treatment such as local radiotherapy. The slow-release injection is used for the treatment of various solid tumors.
CN101843656A External medicinal liquor for treating cancer and preparation method thereof The invention relates to external medicinal liquor for treating cancer and a preparation method thereof. The preparation method of the external medicinal liquor comprises the following steps of: crushing three pure natural plant medicaments such as aizoon stonecrop herb, radix gynurae segeti and vietnamese sophora root; charging the medicaments and original juice liquor into a high temperature resisting glass bottle; fermenting the mixture; filtering out medicinal liquid; and adding a little musk. All the components of the external medicinal liquor are mutually matched, and have the effects of activating blood and dissolving stasis, freeing channels and dissipating binds, eliminating toxic materials and drawing out poison, dispersing swelling and relieving pain, strengthening body resistance and dispersing tumor together. The external medicinal liquor can control hyperplasia of cancer cells, prevent diffusion transfer of the cancer cells and make the cancer cells collapse, shed and disappear.
EP2576567A1 Nitroimidazole derivatives The present invention provides novel compounds useful in the treatment and diagnosis of mycobacterial infections. Compounds of the present invention have enhanced biological properties as compared to the related known compounds. The present invention also provides a precursor compound useful in the synthesis of certain compounds of the invention, and a method to obtain these compounds using said precursor compound. Methods of treatment and diagnosis in which the compounds of the invention find use are also provided.
EP1104403B1 Hydroxy pipecolate hydroxamic acid derivatives as mmp inhibitors A compound of formula (I) wherein R?1, R2 R3, R4 R5, R6, R7, R8, R9¿ and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, and other diseases characterized by matrix metalloproteinase or mammalian reprolysin activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
CN103735548A Application of olmesartan medoxomi i to preparation of drugs for preventing cardiac rupture, complication caused by acute myocardial infarction The invention relates to a novel pharmaceutical application of olmesartan medoxomi i, in particular to an application of the olmesartan medoxomi i to preparation of drugs for preventing cardiac rupture, complication caused by acute myocardial infarction. According to the pharmaceutical application, the olmesartan medoxomi i can be used for effectively preventing cardiac rupture, complication caused by acute myocardial infarction, is favorable for reducing the fatality rate of patients and has a positive clinical meaning. Especially, the olmesartan medoxomi i is used for clinically treating other cardiovascular diseases in addition to the cardiac rupture, and is proved to be safe. Based on the application, the olmesartan medoxomi i can be expectedly used for clinically preventing and treating new indications of the cardiac rupture, complication caused by acute myocardial infarction.
WO2010067233A1 1,2,4 triazolo [4, 3 -a] [1,5] benzodiazepin-5 (6h) -ones as agonists of the cholecystokinin-1 receptor (cck-ir) This invention relates to CCK-1 R agonists of Formula (I) wherein R1-R5 and X are as defined in the specificiation, as well as pharmaceutical compositions containing the compounds and methods of use of the compounds and compositions. The compounds are useful in treating obesity, type 2 diabetes and associated diseases.
WO2010029913A1 Mental vigor improver Disclosed is a mental vigor improver which can improve diminished mental vigor caused by stress or mental fatigue, can also improve diminished volition, diminished attention/concentration, decreased workability or the like, and is safe for oral ingestion. Specifically disclosed is a mental vigor improver comprising at least one flavonoid and/or transglycosylated flavonoid as an active ingredient.
WO2009101959A1 Novel compound, lachnochromonin compound Disclosed is a novel compound having a therapeutic and/or prophylactic activity on inflammatory diseases, lifestyle-related diseases and adult diseases. Specifically disclosed are: a compound represented by general formula (I) [wherein R1 represents CH3; R2 represents OH; R3 represents H; R4 represents CH3; and R5 represents CH(CH3)(CH2)2OH, CH(CH3)CH(OH)CH3 or CH(CH3)CH2CH3]; and others.
WO2008000484A1 Verfahren zur herstellung von pentamethylen-1,5-diisocyanat Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung von Pentamethylen- 1,5-diisocyanat, so hergestelltes Pentamethylen-1,5-diisocyanat und dessen Verwendung.
US20070243222 Fungicidal formulation and method of use A method for treating onychomycosis of a nail of an animal, which comprises a topical application of a solution to said nail, wherein said solution is comprised of at least one chemical agent capable of chelating iron metal ions
CN102964339A Novel pharmaceutical salt of lapatinib The invention relates to a novel pharmaceutical salt of lapatinib. The novel pharmaceutical salt of lapatinib is shown in the figure in the specification, wherein x is 1, 2, or 3, n is 0, 0.5, 1, 1.5, 2, 2.5 or 3, and R is oxalic acid, maleic acid, citric acid, hydrogen bromide, hydrochloric acid, benzene sulfonic acid, p-toluenesulfonic acid, sulfuric acid, methylsulfonic acid, acetic acid, propanoic acid, malonic acid, gluconic acid, succinic acid, fumaric acid, lactic acid, tartaric acid, malic acid, pyruvic acid, hydroxybutyric acid, adipic acid, salicylic acid, phthalic acid or mandelic acid.
US20080139631 3-(2-methyl-4-(trifluoromethyl)-5-cyano-indol-1-yl-methyl)-5-(3-(trifluoromethyl)phenyl)-1,2,4-oxadiazole or salt thereof; hypogonadism, sarcopenia, osteoporosis, wasting diseases, cancer cachexia, frailty, prostatic hyperplasia, prostate cancer, breast cancer; selective androgen receptor modulators This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.
WO2011160845A3 Oxidized phospholipids and lipoproteins, and antibodies thereto, as biomarkers of inflammatory conditions and methods of treatment A method is disclosed for assessing the risk of developing inflammatory conditions, and/or the risk of mortality related thereto, comprising monitoring and/or determining the levels of one or more oxidized phospholipids and lipoproteins, and antibodies thereto, and comparing said levels with predetermined cutoff values, as well as a kit for implementing the method. Also disclosed is a method for treating or decreasing the risk of developing inflammatory conditions, and/or the risk of mortality related thereto, by administering medicaments comprising annexin A5 and/or antibodies to one or more oxidized phospholipids and lipoproteins, as well as bioactive components and/or parts/fragments thereof. Compositions comprising one or more inhibitors of oxidized phospholipids and lipoproteins, as well as bioactive components and/or parts/fragments thereof, as well as compositions comprising one or more conjugates of oxidized phospholipids and lipoproteins, as well as bioactive components and/or parts/fragments thereof, are also disclosed.
US20110300245 Topical, palatable, anti-inflammatory and analgesic for specific application to intraoral, gingival and extraoral areas correlated with, and related to, the trigeminal nerve and its nerve branches and plexus. To mitigate, attenuate or prevent migraine-type headache, cluster-type headache, tension-type headache, post-traumatic headache, atypical facial pain and cervical muscle spasm as well as other idiopathic head or facial pain or discomfort, associated with, or exacerbated by, inflammation The invention is a new unique, palatable, topical, anti-inflammatory and analgesic designed around a specific set of painful conditions, with specifically designated applications, using a different methodology and formulation, with no NSAIDS, steroids or salicylites, than the prior art for this specific set of painful conditions. Thus creating an improved dissimilar system, preventing the prior arts required invasive, costly and inefficient medical procedures, and with a unique lack of negative effects when compared with the prior art. Thereby, facilitating an anti-inflammatory analgesic effect to areas correlating or relating to the trigeminal nervous system, both intraoral and extraoral. Trigeminal tenderness is noted consistently in many painful conditions and this invention can be used to mitigate these areas of tenderness and inflammation preventing or relieving, migraine, cluster-type headaches, tension-type headache, post-traumatic headache, atypical facial pain and cervical muscle spasm as well as other related pain or discomfort exacerbated by trigeminal inflammation.
WO2010091198A1 Therapeutic compositions comprising monoterpenes This invention provides compositions for transport of a therapeutic agent. The compositions contain a therapeutic agent and a monoterpene or an analog thereof. In one aspect, the monoterpene is perillyl alcohol (POH) or an analog thereof. In another aspect, the therapeutic agent is provided in an amount effective to treat the disease or subject of choice.
WO2013062333A1 Composition comprising syringaresinol for improving the skin The present invention relates to a composition for improving the skin, which comprises the compound of chemical formula 1, the derivatives thereof, or the pharmaceutically acceptable salts thereof as active ingredients.
EP1951678A1 Pyrazole compounds having cannabinoid receptor (cb1) antagonizing activity The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: -N(R7)-, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: -N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: -N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.
US20080262025 Processes for the Preparation of Zolpidem and its Hemitartrate The invention relates to the preparation of a non-hygroscopic polymorphic form of zolpidem hemitartrate, designated as Form I, and pharmaceutical compositions including it. The invention also relates to use of the compositions for treating anxiety, sleep disorders and convulsions. The invention also relates to a process for the preparation of zolpidem or pharmaceutically acceptable salts thereof by condensing 3-bromo-N,N-dimethyl-4-oxo-4-p-tolyl-butyramide with 2-amino-5-methylpyridine in a polar aprotic solvent.
US20110142911 HIV epitopes and pharmaceutical composition containing same The invention concerns a peptide comprising an epitope consisting of a sequence of amino acids selected among SEQ ID NO 1, SEQ ID NO 2, SEQ ID NO 3, and having a length not more than 24 amino acids.
WO2008129303A2 Sustained release We describe a medicament for the treatment of thyroid disorders that typically result from a hypoactive thyroid gland that releases thyroxine and triiodothyronine in a sustained pattern when administered to a subject.
CN101023893A Endoluminal device for treating disease of aneurysm and combination of drugs Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Medical devices include stents, grafts, anastomotic devices, perivascular wraps, sutures and staples. In addition, various polymer combinations may be utilized to control the elution rates of the therapeutic drugs, agents and/or compounds from the implantable medical devices.Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic drugs, agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the formation of blood clots. The drugs, agents, and/or compounds may also be utilized to treat specific diseases, including vulnerable plaque. Therapeutic agents may also be delivered to the region of a disease site. In regional delivery, liquid formulations may be desirable to increase the efficacy and deliverability of the particular drug.
EP1137413B1 Non-peptide antagonists of glp-1 receptor and methods of use Non-peptide compounds that act as antagonists of the intestinal hormone glucagon-like peptide 1 (GLP-1) have a 9H-β-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.
WO2005116018A1 TYROSINE DERIVATIVES SUBSTITUTED BYALKANOYLAS hPPARα & hPPARϜ ANGONISTS The invention provides compounds of the general formula (I), racemic mixtures, optical isomers, pharmaceutically acceptable salts, solvates and pharmaceutical compositions thereof. The definitions of substituents in the general formula (I) are the same as the definitions of claims. The present invention also relates to the preparation for the compounds of the general formula (I) and the usage thereof for the preparation of a medicament, which is used for treating hyperglycemia, lipidosis lipaemia and NIDDM (type II) diabetes including diabetes involving lipidosis lipaemia.
US20080249072 Use of Low Dose Chemically Modified Tetracylines to Reduce Inflammatory Mediators The invention is a method for reducing the production of inflammatory mediators, and/or treating conditions characterized by increased levels of inflammatory mediators, in a mammal in need thereof, by administering a 4-dedimethlaminosancycline to the mammal.
CN101756957B Pharmaceutical composition containing artemisinin, artemisinin derivatives and histon deacetylase (HDAC) inhibitor and application thereof The invention relates to a pharmaceutical composition containing artemisinin, artemisinin derivatives and a histon deacetylase (HDAC) inhibitor and an application thereof to prepare medicines for treating intestinal cancer, liver cancer, lung cancer, kidney cancer, gastric cancer, brain tumor, sarcoma, pancreatic cancer, ovarian cancer, breast cancer, prostate cancer or leukaemia. The pharmaceutical composition of the invention has obvious synergistic effect, thus improving curative effect of medicines, lowering administration dosage and reducing occurrence of side effect.
US20090011047 Pharmaceutical compositions comprising of arsenous acid, its sodium salt and its derivatives intended for the treatment or urogenital cancer and its metastasis The present application relates to pharmaceutical compositions and methods for treatment of urogenital diseases and bone metastasis in a human, which pharmaceutical composition contains an effective amount of arsenous acid alkaline or earth alkaline metal salt and/or a pharmaceutically acceptable adjuvant. According to the present invention, the alkaline arsenous acid metal salt is sodium meta-arsenita (AsO2Na) or potassium meta-arsenite (AsO2K). The effective amount of arsenous acid alkaline or earth alkaline metal salt is 0.0001-1500 mg/kg, preferably 1-1000 mg/kg, more preferably 1-150 mg/kg, and most preferably 50-100 mg/kg of body weight/day. The administration form of the pharmaceutical compositions of the invention is preferably oral, such as a tablet, capsule, powder and/or solution with a pharmaceutically acceptable carrier, diluent or excipient.
CN102846564A A cefprozil tablet and its preparation method The invention discloses a cefprozil tablet and its preparation method. The invention aims at the disadvantages of heat- and moisture-instability of cefprozil, and can provide a cefprozil tablet by enhancing the stability of cefprozil through micropellet package and increasing the compacting property. The invention also discloses a pelletization by cold-process dry pelletization, in which the pressing roller is cooled in the pressing process through water circulation (the interior of the pressing roller will not contact the materials) so that the materials will not contact moisture or high temperature during the whole production process so as to ensure the stability and curative effect of cefprozil drug.
CN103709052A Rhein amino-alcohol ester type compound, and preparation method and pharmaceutical application thereof The invention relates to the field of pharmaceutical chemistry and pharmacotherapy and specifically relates to a rhein amino-alcohol ester type compound, and a preparation method and application in pharmaceuticals. The compound has an anti-tumor effect and can be used for preparing anti-tumor medicaments. The invention further relates to the preparation method of the compound.
EP1262181B1 Use of isothiazole derivatives as urease inhibitors for the treatment of helicobacter pylori induced gastrointestinal diseases Urease inhibitors and drugs against Helicobacter pylori which contain, as the active ingredient, isothiazole derivatives represented by the following general formula (1) wherein R1 represents hydrogen or amino; R2 represents hydrogen, lower alkyl or acetyl; and X represents carbon or nitrogen. These drugs are efficacious in preventing and treating gastrointestinal diseases caused by urease of Helicobacter pylori such as chronic gastritis and gastroduodenal ulcer.
CN1660092A Injection preparation of sodium lansoprazole and preparing method A freeze-dried injection of lansoprazole sodium is proportionally from lansoprazole sodium, excipient, pH regulator and antioxidizing agent. Its preparing process is also disclosed.
US20070161681 Ether derivatives useful as inhibitors of pde4 isozymes Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of the formula: wherein the substituents are as defined in the specification.
WO2008096149A2 Napadisylate salt of a muscarinic m3 antagonist The invention provides [2-(4-chloro-benzyloxy)-ethyl]-[2-((R)-cyclohexyl-hydroxy- phenyl-methyl)-oxazol-5-ylmethyl]-dimethyl-ammonium napadisylate, pharmaceutical compositions containing it, and its use in therapy.
WO2014151682A1 Pyrimidine compounds as kinase inhibitors This disclosure relates to compounds, methods for their preparation, pharmaceutical compositions including these compounds and methods for the treatment of cellular proliferative disorders, including, but not limited to, cancer.
WO2011163518A1 Pyrazolo [1, 5 -a] pyrimidines as antiviral agents The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
US7427608 Protection against and treatment of hearing loss The present invention provides a method for protecting against or treating hearing loss in a subject. This method involves administering an effective amount of a protein tyrosine kinase inhibitor to the subject to protect against or to treat hearing loss.
CN101808654B Compounds extracted from palm oil mill effluent for the treatment of cancer, compositions thereof and methods therewith The present invention describes a composition and methods for prevention and treatment of cancer comprising compounds extracted from Palm oil mill effluent. Also, the invention describes effective therapeutic dosages of the compounds and their combinations. The present invention can be prepared independently or as a combination product.
CN101756952A Drug composition of meclofenoxate hydrochloride and polyethylene glycol and preparation method thereof The invention belongs to the technical field of medicine, and discloses a drug composition of meclofenoxate hydrochloride and polyethylene glycol and a preparation method thereof. The weight ratio of the meclofenoxate hydrochloride and the polyethylene glycol is 1:0.002-0.1. The invention solves the problems that the meclofenoxate hydrochloride is easily hydrolyzed when meeting water and instably stored in the prior art. The drug composition has stable property and convenient storage, and improves the safety of clinical medication.
CN101904874A Medicinal composition having effect of enhancing immunologic functions The invention belongs to the technical field of medicine or food. The invention discloses a medicinal composition having the effect of enhancing immunologic functions. The medicinal composition is characterized by comprising the following materials in part by weight: 1 to 500 parts of fermented cordyceps fungi powder and 3 to 20 parts of astaxanthin. Pharmacodynamic experiments show that the medicinal composition has better pharmacological effects than the fermented cordyceps fungi powder or the astaxanthin which are separately used.
WO2013013240A3 Macrocyclic compounds and related compositons and methods of use Compounds and compositions, which can be use for example, for treating cancer, are described herein.
WO2013027806A1 Pharmaceutical composition for preventing or treating underactive bladder Underactive bladder is such a clinical condition that urination disorder is developed as the result of the reduction in contraction of a detrusor muscle (a detrusor muscle of the bladder) during urination, is characterized by the feeling of having to urinate immediately, and is different from overactive bladder. The present invention provides a pharmaceutical composition useful for the prevention or treatment of underactive bladder. The present invention relates to a pharmaceutical composition for preventing or treating underactive bladder, which contains silodosin or a pharmacologically acceptable salt thereof as an active ingredient. This pharmaceutical composition has an effect of improving the urinary flow rate, an effect of improving the overdistension of the bladder (an effect of reducing a bladder capacity) and an effect of improving residual urine, and is therefore useful for the prevention or treatment of underactive bladder.
CN1813761A Combined powder for injection and its preparing method The present invention provides a compound powder injection and its preparation method. It is made up by using cephalosporin antibiotic cefpiramide sodium and beta-lactamase inhibitor sulbactam through a certain preparation process. Said injection preparation has good stability, and can obtain high antimicrobial effect.
US20080255070 Bisphosphonate Compounds and Methods with Enhanced Potency for Multiple Targets including FPPS, GGPPS, AND DPPS The disclosure provides, inter alia, novel bisphosphonate compounds and methods of making and using such compounds. In certain embodiments, compounds of the invention include bisphosphonates that are capable of selectively inhibiting one or more of farnesyl diphosphate synthase (FPPS), geranylgeranyl diphosphate synthase (GGPPS), and decaprenyl pyrophosphate synthase (DPPS). In preferred embodiments, compounds of the invention are capable of selectively inhibiting two or more of FPPS, GGPPS, and DPPS. In embodiments, compounds and methods of the invention demonstrate superior activity levels, such as in the anti-cancer context, immunostimulation context, and other contexts, which in several cases exceed the activity levels of previous generation bisphosphonate drugs by orders of magnitude. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor or cancer cell growth inhibition, activation of gammadelta T cells, inhibition of certain enzymes related to the mevalonate metabolic pathway, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases.
EP0938486B1 Substituted pyrrolopyrimidines and processes for their preparation There are described 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula (I) in which the substituents are as defined in claim 1. These compounds inhibit the tyrosine kinase activity of the receptor for the epidermal growth factor (EGF) and c-erbB2kinase and can be used as anti-tumour agents.
CN103417512A Amoxicillin capsule and method for preparing same The invention discloses an amoxicillin capsule and a method for preparing the same. Medicated granules and lubricants are uniformly mixed with one another and then are filled into a capsule shell to form the amoxicillin capsule which is a preparation. The medicated granules comprise, by weight, 1 part of amoxicillin and 0.1-0.5 part of tartaric acid, and the amoxicillin and the tartaric acid are uniformly mixed with each other and then are granulated by a wet process to obtain the medicated granules. The amoxicillin capsule and the method have the advantages that the capsule can be dissolved out quickly and is good in stability and simple in preparation technique, and the quantity of the types of accessories is low.
WO2008149177A2 Marine lipid compositions and uses thereof Novel marine lipid compositions comprising triglycerides and omega-3 rich phospholipids are described. The compositions are characterized by providing highly bioavailable omega- 3, increased tissue incorporation of omega-3 and reduced concentration of pro- inflammatory cytokines.
CN202537977U Taxol injection The utility model relates to taxol injection, which is characterized by consisting of a syringe and taxol solution sealed in the syringe, wherein the taxol injection can be directly injected into physiological saline, 5 percent glucose injection or 5 percent glucose physiological saline to be diluted and then statically dripped, and a process of cutting an ampoule open to suck into the syringe or sucking into the syringe from a penicillin bottle is avoided, so that the need of for contact of a nurse and the taxol injection is reduced, and the health of the body of the nurse is favorably protected.
WO2009147681A1 Pharmaceutical compositions for treatment of parkinson's disease Pharmaceutical compositions are provided for treatment of Parkinson's disease comprising a pharmaceutically acceptable carrier and a fixed dose combination of two active agents selected from compounds having either neuroprotective or symptomatic effects, or both, in Parkinson's disease patients, wherein the molar ratio of the two compounds is in the range of 1:1 to 1:100. The compositions are formulated for immediate release, controlled release, or both immediate and controlled release
EP1680417A1 1-'(e)-2-(phenyl)ethenyl-4-(arylalkoxy)-oxazole or -thiazole compounds as her-2 tyrosine kinases inhibitors and their use in the treatment of cancer Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms thereof, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
EP1725567B1 Spirocyclic cyclohexane derivatives with affinity to the orl-1 receptor The invention relates to spirocyclic cyclohexane derivatives, to a method for the production thereof, to medicaments containing said compounds and to the use of spirocyclic cyclohexane derivatives for the production of medicaments.
US8309103 synergistic mixture; lower dosage; side-effect reduction The present invention refers to a treatment for mixed infectious diseases in the human reproductive system, wherein an association of compounds containing fluconazole and either tinidazole or secnidazole is used, the same being associated in doses lower to those commonly used therapeutically. The combination has proven to be highly efficacious and shown a good degree of tolerance.
CN101397244B Anti-tumor diterpenoid isoeuphpekinensin in euphorbia perkinensis root and extraction method thereof The invention discloses an anti-tumor diterpenoid compound isoeuphpekinensin which is separated from euphorbia roots, the chemical structure is as the following formula, the chemical structure and the spatial configuration of the compound are determined via the spectral analysis, the integrated analysis of nuclear magnetic resonance spectroscopy and the X-ray single crystal diffraction technology particularly. The preparation method is as follows: the fresh euphorbia root is cut into slices and dried, then ethanol is used for reflux extraction, the ethanol is recycled under reduced pressure, a liquid extract is obtained, and then the chromatographic separation is carried out on the liquid extract by a silica gel column, thereby obtaining the compound. In vitro anti-tumor experiments show that the compound has significant inhibition effect on human nasopharyngeal carcinomas cells, KB cells and others which are six types of tumor cell lines in total. The invention provides the lead compound for developing new anti-tumor medicaments, thereby having important significance on developing and utilizing medicinal plant resources of China.
CN103638530A Alginic acid-adriamycin amycin bonding medicine and preparation method thereof The invention provides an alginic acid-adriamycin amycin bonding medicine which has a structure shown in a formula (I) or (II), wherein n is degree of polymerization of alginic acid, and n is greater than or equal to 7 but less than or equal to 1507. The alginic acid-adriamycin amycin bonding medicine is prepared by taking alginic acid, sodium cyanoborohydride and adriamycin amycin as raw materials. As the raw material alginic acid ahs good bioactivity and biocompatibility, the alginic acid-adriamycin amycin prepared has good bioactivity and biocompatibility. Meanwhile, alginic acid and adriamycin amycin are connected through oxime bonds, and can be quickly released in a tumor tissue or cell under a lower pH value condition, so that the pesticide effect is enhanced. The reductive alginic acid-adriamycin amycin bonding medicine with the structure shown in the formula (II) further has a more stable performance, is more slowly to release adriamycin amycin, and reaches an ideal long-acting treatment.
US20090149413 RORS as Modifiers of the p21 Pathway and Methods of Use Human ROR genes are identified as modulators of the p21 pathway, and thus are therapeutic targets for disorders associated with defective p21 function. Methods for identifying modulators of p21, comprising screening for agents that modulate the activity of ROR are provided.
CN103393755A Natural medicine extract as well as preparation method and application thereof The invention relates to natural medicine extract as well as a preparation method and an application thereof. The natural medicine extract is composed of a water decocted concentration extract of schisandra chinensis and semen raphani, schisandra chinensis polysaccharide and sulforaphane at a ratio of (4-6):(5-9):(3-5), and the natural medicine extract composition has an unexceptionable curative effect on diarrhea related to cancer chemotherapy and meanwhile has a synergistic effect on cancer chemotherapy.
WO2014078633A1 Methods for treating cancers having brca2 and palb2 mutations The present invention provides a method for treating or preventing cancer in a subject wherein the subject is identified as having a BRCA2-/- and/or PALB2-/- mutation comprising: a) obtaining a sample from a subject; b) analyzing the sample for the presence of a BRCA2-/- and/or PALB2-/- mutation; c) administering to the subject a therapeutically effective amount of an C1-C6 aldehyde or prodrug or derivative thereof when the analysis of the sample of b) indicates the subject has a BRCA2-/- and/or PALB2-/- mutation. In addition, the use of a pharmaceutical composition comprising a therapeutically effective amount of an C1-C6 aldehyde or prodrug or derivative thereof, and/or an aldehyde dehydrogenase inhibitor is also provided for treating cancer in a subject wherein the subject is identified as having a BRCA2 -/- and/or PALB2 -/- mutation. Also provided herein is an isolated human adenocarcinoma cell line genetically modified to have a biallelic disruption of the PALB2 gene, and methods for identifying a compound or small molecule that modulates a function of a cancer cell or population of cells genetically modified to have a biallelic disruption of the PALB2 gene are also provided.
EP1348706B1 Substituted thiazole derivatives bearing 3-pyridyl groups, process for preparing the same and use thereof Pharmaceutical compositions which have steroid C17,20 lyase inhibiting activity and are useful as preventive or therapeutic agents for prostatism or tumors such as breast cancer, more particularly, steroid C17,20 lyase inhibitors characterized by containing a compound of the general formula (I) or a salt or prodrug thereof, wherein A1 is an optionally substituted aromatic hydrocarbon group or an optionally substituted heterocyclic group; and one of A2 or A3 is hydrogen, halogeno, an optionally substituted C¿1-4? aliphatic hydrocarbon group, or optionally esterified carboxyl, and the other is an optionally substituted heterocyclic group, with the proviso that at least one of A?1, A2, and A3¿ is optionally substituted 3-pyridyl.
CN101574345A Compound simvastatin niacin sustained release tablet and preparation method thereof The invention discloses a compound simvastatin niacin sustained release tablet and a preparation method thereof. The compound simvastatin niacin sustained release tablet consists of the following four components: (1) a tablet core containing niacin; (2) an isolation layer; (3) a simvastatin layer; and (4) a protective film-coat layer. In the compound preparation, the niacin serves as a sustained release component and the simvastatin serves as a quick release component, thus all components play a synergistic action in vivo to comprehensively adjust the components of blood fat so as to play the drug action to the utmost extent, reduce the toxic side effects of the medicaments, reduce the fluctuation of the blood concentration in vivo, and reduce the dosing frequency of a patient; and the compound simvastatin niacin sustained release tablet is applicable to treating hypercholesteremia and mixed dyslipidemia.
CN1593435A Sustained release/controlled release medicine for treating high blood fat The invention discloses a sustained release/controlled release medicine for treating high blood fat with total gynostemma pentaphylla glycosides as the active constituent, and comprises active constituent 35-85 wt. parts, medicament release retarding agent 10-40 wt. parts, medicament release promoter 0-15 wt. parts, and other auxiliary material components.
US7504409 Chronic obstructive pulmonary disease; asthma; respiratory system disorders; administering 2-aminonicotinic acid, anthranilic acid, bendroflumethiazide The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases.
US7378398 Administering a sulfoquinovosylacylglycerol; uterine cancer, breast cancer or pancreas adenocarcinoma cancer A method for treating an adenocarcinoma excluding colon cancer, lung cancer and gastric cancer, comprising administering to a subject in need thereof and suffering from adenocarcinoma cancer, a pharmaceutically effective amount of at least one sulfoquinovosylacylglycerol compound represented by formula (1): wherein R101 represents an acyl residue of an unsaturated higher fatty acid, and R102 represents a hydrogen atom, and/or at least one pharmaceutically acceptable salt thereof.
EP1017353B1 Therapeutic process for inhibiting nf-kappa b A therapeutic process is provided for the inhibition of NF-λB in mammals in whose cells NF-λB has been activated by an agency external to said cell.
US8784796 Vaccine immunotherapy for treating hepatocellular cancer in immune suppressed patients A method for overcoming mild to moderate immune suppression includes the steps of inducing production of naive T-cells and restoring T-cell immunity. A method of vaccine immunotherapy includes the steps of inducing production of naive T-cells and exposing the naive T-cells to endogenous or exogenous antigens at an appropriate site. Additionally, a method for unblocking immunization at a regional lymph node includes the steps of promoting differentiation and maturation of immature dendritic cells at a regional lymph node and allowing presentation of processed peptides by resulting mature dendritic cells, thus, for example, exposing tumor peptides to T-cells to gain immunization of the T-cells. Further, a method of treating cancer and other persistent lesions includes the steps of administering an effective amount of a natural cytokine mixture as an adjuvant to endogenous or exogenous administered antigen to the cancer or other persistent lesions.
CN102697799A Injection for clearing heavy metals from human body The invention relates to the technical field of medicine, in particular to injection for clearing heavy metals from human body. The injection for clearing the heavy metals from the human body comprises ethylene diamine tetraacetic acid (EDTA), adenosine triphosphate (ATP), coenzyme A (CO-A), Vit B6mg and inosine in certain quantity and ratio. The injection is injected to the human body to form an efficient heavy metal chelating agent for powerfully chelating harmful heavy metals such as lead and mercury and expelling the harmful heavy metals from systems of internal organs, bones, nerves, blood and the like, so that the heavy metals in the human body can be cleared, the body is not injured, loss of nutritional elements such as calcium is avoided, immunity and oxidation resistance of the body are improved, cell membranes are repaired, functions of the internal organs are improved, and various diseases caused by the heavy metals are prevented.
CN103356687A Use of ivermectin and its derivative The invention relates to an ivermectin, and especially relates to a use of ivermectin and its derivative. The ivermectin is a derivative of macrolide avermectin generated by Streptomycete, and the use is an application of the ivermectin and its derivative in the preparation of medicines for treating Farnesoid X receptor mediated bile obstruction, gallstones, non-alcoholic fatty livers, atherosclerosis, inflammations, cancers and the like. The derivative comprises avermectin or doramectin.
CN1593433A Application of agar oligose as a health preserving component Disclosed is the application of agar oligose as a health preserving component, animal and human body tests have shown that agar ligos is a non digestibility oligosaccharide, and has the functions of promoting growth of bifidobacteria, improving human body immunity, and improving internal secretion system.
CN102266308B Method for preparing odor masking sustained-release garlicin composite micro-capsules The invention discloses a method for preparing odor masking sustained-release garlicin composite micro-capsules. In the method, a garlicin/organic attapulgite complex serving as a capsule core is combined with sodium alginate to obtain a complex, and sodium alginate/chitosan micro-capsules are prepared from the obtained complex in a complex coacervation method. In the method, odor is masked and the medicine carrying capacity and envelop rate of the micro-capsules are improved by utilizing the adsorptive power and appetency of organic attapulgite on garlicin; gastric mucosae are protected against the irritation of the garlicin by utilizing the pH dependence of calcium alginate and the protective effect of attapulgite mucosae, and the micro-capsules become enteric medicine carrier materialsunder the synergistic action of the garlicin and the attapulgite on germs in intestinal tracts. In addition, the release of medicines in the micro-capsules is retarded by utilizing the detention effect of the attapulgite on the garlicin and the sustained-release performance of chitosan to improve the sustained-release performance of the micro-capsules. The preparation method is simple and environment-friendly, and can be used for sustained-release carrier materials of various medicines.
EP2697221A1 N- cyclobutyl - imidazopyridine - methylamine as trpv1 antagonists A compound of formula (I) wherein X represents a H atom, or a CH2OH group, Y represents a H atom, or a CH2OH group, but X and Y are not both CH2OH groups and Ar is selected from formulae (IA) and (IB) or a pharmaceutically acceptable salt thereof, useful as TRPY1(VR-1) antagonists.
CN103393894A Tinea relieving powder The invention relates to a tinea relieving powder, which is composed of the following raw materials by weight: 20-30 parts of Radix Sophorae Flavescentis, 15-25 parts of Radix Paeoniae, 10-20 parts of coptis, 5-10 parts of smoked black soil, 10-15 parts of Japanese ampelopsis root, 8-12 parts of fructus cnidii, 10-20 parts of banana peel, 5-10 parts of garden burnet, 15-20 parts of honeysuckle, 8-12 parts of Chinese blister beetle, 4-7 parts of Carpesium abrotanoides, 5-10 parts of broom cypress fruit, 3-6 parts of aloe, 5-8 parts of Lithospermum, 10-15 parts of yellow lead, 15-25 parts of eel bone, 10-20 parts of oleander leaves, 5-10 parts of golden larch bark, 6-12 parts of coconut shell, 4-8 parts of camphor and 10-15 parts of borneol. The powder provided by the invention has reasonable formulation, has main effects of clearing heat, detoxicating, dispelling wind, arresting itching, invigorating blood circulation, relaxing veins, astringing sores, engendering flesh, and repairing skin functions, and auxiliary effects of removing evils and fighting poisons with poisons, thereby reducing the stimulation and side effects of drugs on human skin. The medicines employed by the invention have effects of clearing heat, detoxicating, killing helminth, relieving itching, cooling blood to stop bleeding, promoting blood circulation, relaxing veins, relieving stasis and detoxicating, thereby repairing skin functions from inside to outside.
US7105556 Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
WO2009020270A1 Delivery system for nucleic acids using cationic polymer conjugates The present invention relates to a delivery system for nucleic acid using a cationic polymer conjugate, and more specifically relates to a delivery system for nucleic acid comprising a cationic polymer conjugate prepared by conjugating hyaluronic acid or its derivative and polyethyleneimine, and a composition of delivering a nucleic acid into mammalian cell comprising a complex of the nucleic acid and a cationic polymer conjugate with electrostatic binding.
US20090047279 (R)-N-Stereoisomers of 7,8-Saturated-4,5-Epoxy-Morphinanium Analogs Novel (R)—N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the (R)—N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs and methods for their pharmaceutical uses are also disclosed. Such analogs are disclosed as being useful in treating, among varying conditions, opioid-induced constipation.
US20100183654 Immunoreactive protein orthologs of ehrlichia canis and e. chaffeensis The present invention concerns gp36 immunoreactive compositions for E. canis and gp 47 immunoreactive compositions for E. chaffeensis. In particular, epitopes for E. canis gp36 and E. chaffeensis gp 47 are disclosed. In certain embodiments, the immunoreactive compositions comprise tandem repeats having carbohydrate moieties.
US20120082636 Stabilized alpha helical peptides and uses thereof Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.
US20130064891 Pharmaceutical compositions of nsaid and acid inhibitor The present invention relates a pharmaceutical composition comprising esomeprazole magnesium dihydrate, non-steroidal anti-inflammatory drug and one or more pharmaceutically acceptable excipients, wherein non-steroidal anti-inflammatory drug is present in two or more portions. More particularly, the invention relates to compositions comprising Esomeprazole and Naproxen and a process for preparation thereof. Further invention relates to a pharmaceutical composition comprising esomeprazole magnesium dihydrate, non-steroidal anti-inflammatory drug and one or more pharmaceutically acceptable excipients wherein, esomeprazole magnesium dihydrate and non-steroidal anti-inflammatory drug provides co-ordinated release.
EP2687210A1 Stimulators and activators of soluble guanylate cyclase for use in the treatment of sickle cell anaemia and preservation of blood substitutes Use of stimulators and activators of soluble guanylate cyclase (I) for treating sickle-cell anemia and for conserving blood substitutes, is claimed. ACTIVITY : Antianemic; Antisickling; Hypotensive; Antianginal; Antiarteriosclerotic; Vasotropic; Antiasthmatic; Auditory; Ophthalmological; Nephrotropic; Respiratory-Gen.; Antimigraine; Neuroprotective; Nootropic; Antidepressant; Anti-HIV; Antiinflammatory; Gastrointestinal-Gen.; Antiarthritic; Antirheumatic; Immunosuppressive; Antipsoriatic; Antiseborrheic; Dermatological; Antiparkinsonian. MECHANISM OF ACTION : None given.
EP1384476B1 Azolylcarbynol derivatives of aryl (or heteroaryl) for the treatment of respiratory diseases The invention relates to azolylcarbynol derivatives of aryl (or heteroaryl) of general formula (I), wherein Ar represents an optionally substituted phenyl or thyenyl radical; R1 represents a hydrogen atom or an inferior alkyl group; R2 represents a dialkylaminoalkyl or azaheterocyclilalkyl radical and Het represents a non-substituted azole or an azole optionally substituted by one or two substituents, and their physiologically acceptable salts. Said derivatives are useful as medicaments en human and/or veterinary therapy for the treatment of respiratory diseases, more particularly for the treatment of coughing, bronchitis, chronic obstructive lung diseases, allergic rhinitis and asthma.
CN101982192B Lycium ruthenicum Murr proanthocyanidin product and preparation method thereof The invention relates to a lycium ruthenicum Murr proanthocyanidin product. The product is a pale purple pink powder product which is prepared from fresh lycium ruthenicum Murr as raw materials and contains 40% to 70% of oligomeric proanthocyanidins, 10% to 35% of high polymer procyanidins, and 10% to 40% of other impurities after being separated and purified. The invention also discloses a preparation method of the product. The invention adopts the membrane separation technique, has simple and quick method, not only avoids using toxicant organic reagent and acquires the product having stableand uniform property, but also efficiently lowers the producing cost and can adopt the raw materials of health care product which has an antioxidant function.
CN102321129A Stilbene glycoside injection and preparation process thereof The invention adopts stilbene glycoside raw materials for preparing stilbene glycoside injection and belongs to the technical fields of medicinal preparations and a clinical application thereof. The stilbene glycoside is scientifically extracted and refined from plants such as polygonum multiflorum and the like, the injection preparation process technology in the medicine pharmaceutics is applied, the recipe adopting 50 to 100g of stilbene glycoside, 1g of sodium sulfite, 9g of sodium chloride, 50 to 100g of mannitol and 1000ml of distilled water for injection is adopted, the stilbene glycoside is dissolved in the distilled water for injection so that according to the percent weight in volume, the final concentration of the aqueous solution is 5 to 10 percent, 5 to 10 percent of bottle holding agents such as mannitol are added, the PH valve is regulated to 7.0 to 7.2, the filtering and the filter membrane degerming or ultrafiltration are carried out, sterile solution is filled in 10ml pipe bottles, and 4ml sterile solution is filled in each bottle, a freeze-drying method is adopted for removing moisture in the tilbene glycoside, and the powder injection for stilbene glycoside injection is prepared. The stilbene glycoside injection can be used for treating dementia, cerebral apoplexy, coronary heart diseases and angina.
CN1915240A Medication for treating ulcer of upper digestive tract A medicine for treating the ulcer in digestive tract including gastric ulcer and duodenal ulcer with high curative effect is prepared from chitosan.
CN101139350B Oridonin derivative, preparation method and uses thereof The present invention relates to a natural drug and the chemical field of drugs, specifically relating to an oridonin derivative (I); the derivative is the product after the structural transformationof C1 and C14 of the oridonin. The present invention also discloses the preparation method of the oridonin derivatives and the application of the novel oridonin derivative in the anti-tumor field.
WO2010146831A1 Prenatal milk-derived composition for preventing the risk of low birthweight of newborns An object of the present invention is to develop a pharmaceutical composition or a food composition that ameliorates the low birthweight of newborns and prevents the birthweight from decreasing to a level below the average body weight (low body weight at birth) through improvement of nutrients during pregnancy. The present invention provides an agent for preventing low birthweight comprising milk phospholipids as an active ingredient, by which the low birthweight of newborns can be prevented.
WO2013173370A1 Small molecule inhibitors of rna binding motif (rbm) proteins for the treatment of acute cellular injury A method of treating a cellular injury in a subject comprising administering to a subject in need thereof, a therapeutically effective amount of a compound of formula I: wherein at least one of R1 -R8 is a sulfonic acid, a carboxylic acid, a phosphonic acid, a pharmaceutically acceptable salt of a sulfonic acid, a pharmaceutically acceptable salt of a carboxylic acid, a pharmaceutically acceptable salt of a phosphonic acid, a sulfonate ester, a carboxylate acid ester, or a phosphonate ester; and the remaining R1 -R8 are each i·ndependently selected from hydrogen, halo, hydroxyl, nitro, nitroso, amino, substituted amino, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoy, alkenyloxy, substituted alkenyloxy, alkynyloxy, substituted alkynyloxy, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, cycloalkynyl, substituted cycloalkynyl, cycloalkyloxy, substituted cycloalkyloxy, heterocyclyl, substituted heterocyclyl, heterocyclyloxy, substituted heterocyclyloxy, heterocyclylthio, substituted heterocyclylthio, cyano, acyl, acylamino, acyloxy, aminocarbonyl, aminocarbonylamino, aminothiocarbonylamino, aminocarbonyloxy, aminosulfonyl, sulfonylamino, aryl, substituted aryl, aryloxy, substituted aryloxy, arylthio, substituted arylthio, alkylthio, substituted alkylthio, cycloalkylthio, substituted cycloalkylthio, cycloalkenylthio, substituted cycloalkenylthio, thiol, heteroaryl, substituted heteroaryl, heteroaryloxy, substituted heteroaryloxy, heteroarylthio, substituted heteroarylthio, sulfonyl, or sulfonyloxy.
WO2008139152A1 N-oxide-containing pharmaceutical compounds The invention provides a method of preparing a therapeutically active compound having reduced hERG activity, which method comprises: (a) selecting a non-N-oxide drug compound containing a basic tertiary amino group, wherein said non-N-oxide compound is known to have or is suspected of having a therapeutically unacceptable level of hERG inhibitory activity; (b) testing the non-N-oxide drug compound for hERG inhibitory activity; (c) reacting the non-N-oxide drug compound with an oxidising agent to form an N- oxide drug compound having an N-oxide at the basic tertiary amino group; (d) testing the N-oxide drug compound for hERG inhibitory activity; (e) testing the N-oxide drug compound for therapeutically useful activity; (f) comparing the hERG inhibitory activity of the N-oxide drug compound and non- N-oxide drug compound; and (g) when the N-oxide drug compound has therapeutically useful activity and has hERG activity which is at least ten fold less than the hERG inhibitory activity of the non-N-oxide drug compound, formulating the N-oxide drug compound for use in medicine. Also provided by the invention are novel compounds prepared by the aforementioned method and the use of the novel compounds in medicine.
CN1759833A Application of indole-2,3-diketone in preparing medication for antivirus or immunopotenfiator An application of indole-2.3-bione in preparing the antiviral medicine for HIV, influenza virus, hemorrhagic virus and herpes simplex virus and the immunopotentiator is disclosed.
CN101933959A Medicament for treating canker and preparation method thereof The invention discloses a medicament for treating canker. The medicament is prepared from the following raw materials in part by weight: 3 to 17 parts of calcined keel, 3 to 17 parts of calcined oyster, 2 to 16 parts of Chinese gall, 1 to 9 parts of borneol, 0.5 to 7 parts of dried alum and 7 to 24 parts of natural indigo. A preparation method for preparing the medicament for treating the canker comprises the following steps of: crushing the calcined keel, the calcined oyster, the Chinese gall, the borneol, the dried alum and the natural indigo to be 80 and 120 meshes, and preparing the crushed raw materials into powder or suppository. The medicament has the effects of inducing astringency, diminishing inflammation, stopping bleeding, eliminating putridity and engendering the new, dispersing swelling, detoxifying and promoting flesh engendering and wound closing, and has extremely good curative effect on various chronic cankers such as mouth mucosa ulcer, bedsore burst ulcer, trauma non-healing ulcer, ulcer of skin and external diseases, cervical erosion and colpitis and skin surface cankers caused by burn, scald and the like.
EP1633356A1 Treatment of tay sachs or sandhoff diseases by enhancing hexosaminidase activity The invention provides a method for treating an animal suffering from a disease associated with reduced activity of a lysosomal hexosaminidase by administering to the animal an effective amount of a compound which increases the activity of the hexosaminidase.
CN103432507A Medicinal composition for treating hand-foot-mouth disease The invention relates to a medicinal composition for treating hand-foot-mouth disease. The medicinal composition is a preparation prepared from the following medicinal raw materials: ovateleaf holly bark, Chinese date, pawpaw, garlic, mungbean, indigoplant, liquidambar formosana hance, rose, radix tinosporae, Chinese mosla herb, melia toosendan, vine of multiflower knotweed, scorpion, concha haliotidis, platycodon grandiflorum, fructus chebulae immaturus, lophatherum gracile, dayflower, yam, potentilla chinensis, Chinese azalea flower, rhizoma bolbostemmae, dodder, Chinese violet, cockscomb, longan pulp, cortex dictamni, sedum sarmentosum, gordon euryale, mulberry twig, fructus polygoni orientalis, pine nodular branch, humifuse euphorbia herb, loquat leaf, stalactite, chingma abutilon seed, Chinese starjasmine stem, zaocys dhumnade, himalayan teasel root, honeysuckle stem, folium turpiniae, hawthorn, amomum tsao-ko, valeriana jatamansi jones, spina gleditsiae, camuning, lotus stamen, marmor serpentinatum, lindley eupatorium herb, swertia mileensis and Chinese waxgourd peel. The medicinal composition is reasonable in prescription, has definite curative effect, and can be used for effectively treating hand-foot-mouth disease.
CN101366790A Propolis oral liquid and uses thereof The invention discloses propolis oral liquid and application thereof. The propolis oral liquid comprises propolis extract and white wine, and also contains honeysuckle concrete; the weight ratio of the honeysuckle concrete to the propolis extract is 1 to between 1 and 1.2; and the invention discloses the application of the propolis oral liquid in the treatment of acute and chronic pharyngitis, acute tonsillitis and parotitis. Compared with the prior art, the cure rate of the acute and chronic pharyngitis is 91.6 percent, the cure rate of the acute tonsillitis is 95 percent, and the cure rate of the parotitis is 80 percent.
US20120100067 Solubilisation Method The present invention relates to the solubilisation of an active agent in a lipid dispersion, in particular to the solubilisation of an active agent in a suspension of preformed empty liposomes.
WO2007123027A1 Anti-cancer agent comprising cyathane derivative The object is to provide a novel anti-cancer agent having fewer adverse side-effects and more potent anti-cancer activity compared to a conventional anti-cancer agent. It is found that sarcodonin A, which is a cyathane derivative contained in a fruit body of Sarcodon scabrosus, has a potent anti-cancer activity. The anti-cancer activity is particularly prominent in a human esophageal cancer cell and shows little toxicity against a normal human cell. By using sarcodonin A as an anti-cancer agent, it becomes possible to provide a pharmaceutical composition for use as an anti-cancer agent which has few adverse side-effects and a potent efficacy or a beverage/food composition.
WO2011044434A2 A composition and a method of treating cns disorders and hyperpigmentation The present invention relates to a method of treating CNS disorders, particularly Alzheimer's disease. The method comprise step of administering to a subject in need thereof a therapeutically effective amount of hydroxychavicol and/or its derivatives or a composition comprising hydroxychavicol and/or its derivatives optionally along with pharmaceutically acceptable excipients. The invention also relates to use of hydroxychavicol and/or its derivatives for treating hyperpigmentation.
CN103040780A Rapidly disintegrating pramipexole tablet drug composition and preparation method thereof The invention relates to a rapidly disintegrating pramipexole tablet drug composition and a preparation method thereof. The invention particularly relates to a pramipexole tablet which comprises 0.1-2 parts by weight of pramipexole, 20-500 parts by weight of mannitol and calcium hydrophosphate with the weight accounting for 1-50% of that of mannitol. The preparation method of the pramipexole tablet comprises the following steps of sieving materials with a 40-100-mesh sieve, uniformly mixing the materials, and tabletting. The obtained pramipexole tablet has the significant pharmaceutical advantages, such as rapid disintegrating.
US20110212166 Carnitine conjugates of adamantanamines derivatives as dual prodrugs for various uses This invention concerns compounds of adamantanamines and neramexane, including their pharmaceutically-acceptable salts, diesterioisomers, and formulations for treating Alzheimer's related dementias, depression, AIDS related dementias, as antivirals, inflammatory diseases such as rheumatoid arthritis, and cerebral ischemia, hyperlipidemia, and diabetes.
CN101200438A Novel water-soluble azulene derivatives, preparation method and medical composition thereof The invention provides compounds with the structure shown in Formula 1, and these compounds can be used as medicines to gastritis and peptic ulcer; wherein, M is metal ion, including Na, K, Zn, Mg and Bi, n is an integer ranging from 1 to 3 and X is 0, 0.5, 1, 1.5, 2, 2.5 or 3.
CN101503397A Halogenated furan ketone compound, and use thereof in antiinfective drug preparation The invention discloses a halogenated furanone compound and the application thereof in preparing anti-infective drugs. The structural formula of the halogenated furanone compound is indicated by the formula (I), II), (III), (IV), (V), (VI), (VII) or (VIII). The halogenated furanone compound designed and synthesized by the invention has good effect in inhibiting the formation of bacterial biomembranes, can be used as a bacterial biomembrane inhibitor, is separately used or used together with antibiotic drug to overcome the problem of clinical antibiotic resistance.
CN102058876A Cervix antibacterial repair complex and preparation method thereof The invention relates to a cervix antibacterial repair complex and a preparation method thereof. The complex comprises the following raw material components in part by weight: 0.01 to 100 parts of gelatin, 0.01 to 100 parts of water-soluble chitosan, 1 part of bamboo carbon fibers, and 0.1 to 300 parts of acidic aqueous solution. The preparation method comprises the following steps of: adding the gelatin and the water-soluble chitosan into the acidic aqueous solution, fully stirring, adding the bamboo carbon fibers, injecting into a mold, and performing vacuum freeze drying to obtain a dried antibacterial material. The preparation method is simple in formula and feasible, has the characteristics of low temperature, vacuum and energy consumption and environmental friendliness, and meets the requirement of synthesizing the material in a soft processing mode.
CA2573261A1 Compositions for enhancing the production of ppar and/or ppar-associated factors Attention is focused on a nutritional composition known as having an effect of controlling blood glucose level. This food is administered to rats over a long time and the expression of genes relating to the lipid metabolism in the liver and fat tissues of the animals is analyzed by the real time PCR method. As a result, it is observed that the expression of PPAR.alpha. gene is promoted by the above-described food and, in its turn, the expression of fatty acid metabolism-related genes (i.e., PPAR.alpha. target genes) is promoted while the expression of fatty acid synthases is regulated. Moreover, it is confirmed that the above food exerts an effect of promoting the expression of PPAR.gamma. and adiponectin. Thus, it is found out that this food has effects of enhancing the production of PPAR and PPAR-associated factors.
US20100003335 Microparticles for delivery to cells and/or tissue Delivery of bioactive molecules (BAMs) to organelles, cells, tissues, or animals with high efficiency is desirable. Novel compositions for highly efficient delivery of bioactive molecules by biolistic methods are described. The novel compositions include novel microparticle cores, microparticle core/BAM complexes, microparticle core/nanoparticle complexes and multilayer-microparticle core/BAM complexes. Any one of these may be further modified to include targeting agents.
US7479488 Selected CGRP—antagonists, process for preparing them and their use as pharmaceutical compositions The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
EP1963508A2 COMPOSITIONS AND METHODS OF USING siRNA TO KNOCKDOWN GENE EXPRESSION AND TO IMPROVE SOLID ORGAN AND CELL TRANSPLANTATION This invention describes compositions and methods using siRNA to target various genes expressed in cells of transplanted organs or tissues and/or genes expressed in the host to improve the success of the transplantation.
US8513281 Method of treating traumatic brain and spinal cord injuries and other neurogenic conditions using non-steroidal anti-inflammatory drugs and naturally occurring conotoxins A method for treating a patient/subject having neuronal injury, pain, neurotrauma and/or traumatic brain injury, such as diffuse axonal injury, which includes intrathecally and/or intraventricularly administering to the subject a therapeutically effective amount of a non-steroidal anti-inflammatory drug and/or a naturally occurring omega conotoxin, functional fragment thereof, a pharmacologically acceptable salt, ester, amide, or prodrug thereof.
WO2013178821A1 Inhibitors of the notch signalling pathway and secretion for use in medicine The invention relates to dihydropyridine compounds as inhibitors of the notch signalling pathway and/or inhibitors of secretion for the treatment of secretion-dependent disease, such as cancer or senescence-related ageing, in addition to pharmaceutical compositions thereof and methods of treatment.
EP2051961A1 Novel isoindol derivatives as ep4 receptor agonists A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, R4 and R5, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
CN101822817A Compound doxycycline hydrochloride injection for treating intestinal diseases of animals and preparation method thereof The invention discloses compound doxycycline hydrochloride injection for treating intestinal diseases of animals, and the injection comprises principle agent, addition agent and solvent, wherein the principle agent is prepared by the following raw materials in parts by weight: 10-100 parts of doxycycline hydrochloride and 25-250 parts of sulfamethoxazole, or 10-100 parts of mequindox, or 10-100 parts of colistin sulfate, the addition agent is prepared by the following materials in parts by weight: 1-2 parts of antioxidant and 0.1-0.2 part of ethylene diamine tetraacetic acid-2Na, and the solvent is prepared by 650-980 parts of solvent for injection by weight. Clinical tests prove that the compound doxycycline hydrochloride injection for treating intestinal diseases of animals has better treating effects than unilateral preparations which respectively include each medicine and has the characteristics of wide antimicrobial spectrum, strong antibacterial activity, safe use and approval treating effects.
CN102204972A Preparation method of liquid medicine for external use for treating chilblain The invention discloses a preparation method of a liquid medicine for external use for treating chilblain, prepared by soaking cherries in alcohol, burying deeply, taking out and filtering, and adding a small amount of camphor to the filtrate. The liquid medicine disclosed by the invention has the efficacies of preventing and treating chilblain, and simultaneously has the efficacy of treating burn; when the liquid medicine is applied to a burnt area, pain is alleviated quickly, the burnt area can not blister or fester, and the surface of wound heals quickly; and the liquid medicine has convenience in use, a high cure rate and safety in use without any toxic side effects.
CN101229296A Medicine compounds for treating hypertension, heart disease and angina The invention discloses a medicine composition for treating hypertension, heart disease and angina pectoris, comprising blood scorpion, pangolin, leech, storax and borneol. The invention has medicine effects of having human ideas straightened out, inducing resuscitation, relieving blood status for stagnation, activating blood flow, keeping calm and relieving pain, removing pathogenic heat from blood, reducing blood pressure and spasmolysis, and has significant effect in treating various hypertensions, heart diseases and angina pectoris.
US20100215603 Body Surface Protecting Composition A body surface protecting composition, comprising at least one type of multi-chain multiple hydrophilic group-type compound having two or more hydrophobic groups and two or more hydrophilic groups in the molecule, which has an excellent effect of accelerating the recovery of the barrier function of skin and hair and preventing degradation of that function.
US20100029641 Aryl sulfamide derivatives and methods of their use The present invention is directed to aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
US7258871 Combination of a transdermal therapeutic system and an oral and/or parenteral preparation containing dopamine agonists for the treatment of dopaminergic disease states The invention relates to the use of a dopamine agonist in the form of an agent consisting of at least two spatially discrete compositions, of which one is a transdermal therapeutic system (TTS) containing the dopaminergic agent and another one or more are preparations for oral and/or parenteral application containing that same dopaminergic agent for the treatment of dopaminergically treatable diseases with the following elements: a) the TTS is continuously applied, b) within the duration of application in a) the composition for oral or parenteral dosage is administered.
US20080044378 Methods and Compositions for Protein Production Using Adenoviral Vectors The present invention provides methods and compositions for recombinant protein production through replication-defective adenoviral vector infection of non-trans-complementation cell lines. Thus, this invention describes methods of heterologous protein production without an accompanied production of adenoviral vectors.
WO2007072764A1 Ce forming/maturing agent, parakeratosis inhibitor, skin barrier function recovery accelerator, and skincare composition for external application to skin Disclosed is a skincare composition for external application to skin, which contains an imidazole derivative represented by the general formula (1a) or (1b) below and/or a salt thereof in an amount of 0.01-5% by mass relative to the total amount of the composition. (1a) (1b) (In the formulae, R1 represents a hydrogen atom or a methyl group; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents a hydrogen atom, a lower alkyl group or an acyl group.)
US20120282252 5Imidazoquinolines and Pyrimidine Derivatives as Potent Modulators of VEGF-Driven Angiogenic Processes The invention relates to the use of compounds of formula (I) or (II) in the treatment of mammalian target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.
US20110003829 Enrofloxacin hexahydrate The present invention relates to a novel hexahydrate of enrofloxacin, to processes for its preparation, to pharmaceuticals containing it, and to its use in combating diseases.
CN101991817A Brain strengthening and nerve calming medicament The invention discloses a brain strengthening and nerve calming medicament, which is particularly applied to people who are absentminded, stressful, weak and sleepless. The invention provides a brain strengthening and nerve calming medicament, which can gradually improve and restore mental state after long-term application. The brain strengthening and nerve calming medicament is prepared from the following materials: 6 to 12 parts of choerospondias axillaris, 6 to 12 parts of Chinese angelica, 6 to 12 parts of Chinese eaglewood, 6 to 12 parts of corydalis pygmaea, 6 to 12 parts of nutmeg, 6 to 12 parts of emblic leafflower fruit, 6 to 12 parts of longfruit speedwell herb, 6 to 12 parts of garlic, 6 to 12 parts of medicine terminalia fruit, 6 to 12 parts of raisin, 0.1 to 0.8 parts of cinnabar, 6 to 10 parts of cattail pollen, 10 to 20 parts of astragalus root, 3 to 6 parts of Sinkiang arnebia root, 6 to 12 parts of largehead atractylodes rhizome, 4 to 10 parts of atraotydin, 2 to 8 parts of epimedium herb, 5 to 10 parts of eucommia bark, 4 to 10 parts of cassia twig, 2 to 6 parts of lightyellow sophora root, 3 to 8 parts of chrysanthemum, 2 to 6 parts of skunk bugbane, 3 to 8 parts of cynomorium coccineum, 6 to 12 parts of manchurian wildginger, 6 to 15 parts of codonopsis pilosula, 3 to 6 parts of white pepper, 3 to 6 parts of carbonized human hair, 3 to 6 parts of safflower, 6 to 15 parts of dried ginger and 4 to 10 parts of root of rehmannia.
US6987103 Treatment of chronic myelogenous leukmia, resistant or intolerant to ST1571, involving homoharringtonine alone or combined with other agents The present invention concerns a method of treating chronic myelogenous leukemia, a related myeloproliferative disorder or a Ph-positive acute lymphocytic leukemia in a subject animal, comprising: (a) selecting or identifying an animal suffering from chronic myelogenous leukemia or a related myeloproliferative disorder and showing resistance or intolerance to treatment with STI571; and (b) administering to the animal homoharringtonine. In a preferred embodiment, the animal is a human being.
WO2011000566A3 Compounds and pharmaceutical compositions for the treatment of negative-sense ssrna virus infections The present invention relates to novel compounds and pharmaceutical compositions and the use thereof for the manufacture of a medicament for treating, ameliorating, or preventing disease conditions caused by a viral infection with negative-sense ssRNA viruses.
US20120082635 2-amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo- ethanoyl derivatives as potent dpp-iv inhibitors The present invention is related to novel 2-Amino-2-[8-(dimethyl carbamoyl)-8-aza-bicyclo[3.2.1]oct-3-yl]-exo-ethanoyl derivatives of the general formula (A), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors, which are useful in the treatment or prevention of diseases particularly Type II diabetes, other complications related to diabetes and other pathogenic conditions in which DPP IV enzyme is involved.
WO2007064755A2 Treatment of xerostomia with a sulfur-containing antioxidant Xerostomia is treated with a sulfur-containing antioxidant, such as N-acetylcysteine. Delivery compositions including polyoxyalkylene block copolymers may be used, which may be formulated to exhibit reverse-thermal viscosity behavior.
CN1561979A Micro capsule for choline chloride for ruminant stomach and its preparing method A through-rumen microsoftgel choleaevin as feed additive is prepared from the SiO2 carried choleaevin as core and the hydrogenated plant oil as shell through proportionally mixing, and granulating.
US20110256237 Methods and compositions for treating acne vulgaris and acne rosacea Methods and compositions are described for treating acne vulgaris and acne rosacea by administering compositions suitable for oral administration. Suitable compositions contain high dosages of the vitamin nicotinamide combined with much lower dosages of azelaic acid.
EP0946147B1 Composition suitable for the treatment of equine laminitis Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID mixed in a lipid-based carrier are described. The application of such combinations to the affected areas, e.g., the hoofs and surrounding tissues, of an equine afflicted with laminitis provides relief from the debilitating effects of this painful, often life-threatening condition.
CN102048709A Gentamycin sulfate capsule and preparation method thereof The invention relates to a gentamycin sulfate capsule which is prepared by the following raw materials in percent by weight: 20-40 percent of gentamycin sulfate, 20-65 percent of starch, 5-25 percent of calcium sulfate, 0.5-10 percent of microcrystalline cellulose, 0.5-5 percent of hydroxy propyl methyl cellulose and 5-20 percent of lubricating agent. The capsule adds the stability of gentamycin sulfate, also avoids the bitterness of gentamycin sulfate, and increases the compliance of patients.
EP1259259B1 Mucosal adjuvant formulation Adjuvant for mucosal vaccines which modulates the effects of substances, including vaccine antigens in contact with mucosal body surfaces.
US20080119449 Reducing the risk of osteoporotic bone fractures; kit The present invention provides methods for treating physical conditions resulting from postmenopausal estrogen decline in a postmenopausal subject, and in particular methods for reducing the risk of osteoporotic bone fractures in a postmenopausal subject. The present invention also provides a kit useful for carrying out the methods of the present invention.
WO2008109380A3 Nucleic acid compounds for inhibiting vegfr family gene expression and uses thereof The present disclosure provides meroduplex ribonucleic acid molecules (mdRNA) capable of decreasing or silencing one or more VEGFR family gene expression. An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to one or more VEGFR family mRNA. In addition, the meroduplex may have at least one uridine substituted with a 5-methyluridine and optionally other modifications or combinations thereof. Also provided are methods of decreasing expression of one or more VEGFR family gene in a cell or in a subject to treat one or more VEGFR family-related disease.
CN103553996A Anticholinergic pharmaceutical composition The invention relates to an anticholinergic pharmaceutical composition. Specifically, the invention relates to a medicament capable of being used in pharmacy, wherein the,medicament comprises a compound expressed by the following formula. The invention further provides a preparation of the medicament, and the medicament and the preparation are used as an anticholinergic medicament and can be clinically used for anesthesia, peptic ulcer, salivation, etc. The raw material medicament or preparation has the function of inhibiting gastric secretion and regulating gastrointestinal peristalsis; the raw material medicament or preparation has relatively strong salivary secretion resistance than atropine while having no central anticholinergic activity. The anticholinergic pharmaceutical composition is generally used for clinically treating such symptoms as gastric and duodenal ulcer, chronic gastritis and excessive secretion of gastric acid.
US7097851 Multilayer capsule comprises an adhesion site-controlling layer for attaching to a selected site in the intestines, a drug-carrying layer, a protecting layer for preventing from digestive juice; improve bioavailability due to a low absorption in the digestive tract; dosage forms An oral formulation for gastrointestinal drug delivery which comprises an adhesion site-controlling layer for attaching the formulation to the selected site in the digestive tract, a drug-carrying layer for containing a drug and an adhesive and a protecting layer for protecting the drug in the drug-carrying layer, wherein the drug-carrying layer exists between the protecting layer and the adhesion site-controlling layer, and the adhesion site-controlling layer may attach to the protecting layer. The formulation can improve bioavailability of drugs which have low bioavailability.
CN103442710A Combination of checkpoint kinase 1 inhibitors and WEE1 kinase inhibitors A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.
US20110166155 Substituted Isoindolones and Their Use as Metabotropic Glutamate Receptor Potentiators The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
CN1679613A Compound aspartic acid potassium magnesium energy mistura vitamin preparation and use thereof A high-energy composite medicine for treating cardiovascular and cerebrovascular diseases contains proportionally 13 active components including inosine, adenosine triphosphate, VC, potassuim aspartate, magnesium aspartate, VC, VB, etc.
US7304064 1-[(indol-3-yl)carbonyl]piperazine derivatives The present invention relates to 1-[(indol-3-yl)carbonyl]piperazine derivative according to the general formula I or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said 1-[(indol-3-yl)carbonyl]piperazine derivatives, and to the use of these derivatives in the treatment of pain, such as peri-operative pain, chronic pain neuropathic pain, cancer pain, and pain and spasticity associated with multiple sclerosis.
US20070249718 Stable gabapentin compositions Stable compositions containing gabapentin compositions, methods of preparing such compositions, and methods of using such compositions.
US20110015188 Treatment of Seasonal Conditions Multi-dose active agent packages and methods for using the same for treating a subject for a condition are provided. Aspects of the invention include a multi-dose active agent package containing a plurality of unit dosage forms of an active agent configured to modulate at least a portion of a subject's autonomic nervous system during at least one season of the year. The active agent is present in an amount sufficient to alter the parasympathetic activity/sympathetic activity ratio of the subject in a manner effective to treat the subject for the condition. The subject active agent packages and methods find use in the treatment of a variety of different conditions, including disease conditions that increase in severity and/or occurrence during one or more seasons of the year. Also provided are kits for use in practicing the subject methods.
US20100267800 N-Alkyl-Hydroxamic Acid-Isoindolyl Compounds and Their Pharmaceutical Uses The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4.
WO2007132228A1 Combination of cndac with a 2-substituted-4-heter0aryl-pyrimidine amine and use thereof in the treatment of a proliferative disorder A first aspect of the invention relates to a combination comprising CNDAC, or a prodrug thereof, and a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl; R2 and R3 are each independently selected from H and alkyl; and R4 is a heteroalicyclic group optionally substituted by one or more substituents selected from alkyl, CO-alkyl and aralkyl. A second aspect of the invention relates to a pharmaceutical product comprising a compound of formula (I),, or a pharmaceutically acceptable salt thereof, and CNDAC, or a prodrug thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a compound of formula I, or a pharmaceutically acceptable salt thereof, and CNDAC, or a prodrug thereof, to a subject.
US20110184032 Novel Phenylamino Isonicotinamide Compounds The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.
CN103585109A Cefquinome liposome and preparation method thereof The invention discloses cefquinome liposome. The cefquinome liposome comprises the following raw materials by weight: 0.01-50% of cefquinome or a salt thereof, 10-99.99% of phospholipid, 0-65% of cholesterol, 0-60% of deoxysodium cholate, 0-89.99% of anionic lipid, and 0-40% of an antioxidant. The invention further discloses a preparation method of the liposome. The cefquinome liposome researched by the invention has the advantages of excellent packaging rate, uniform particle size distribution, achievement of intravenous injection or local application standards, excellent stability and further improvement of stability through preparation of freeze-dried products. Moreover, the blank liposome-ammonium sulfate gradient medicine carrying preparation technique adopted by the invention is very suitable for large-scale industrial production, and has a wide industrialization prospect.
EP2617722A1 Hetero ring-fused imidazole derivative having ampk activating effect Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is -O-; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
EP2081556A1 Stable imatinib compositions Formulations containing imatinib, preferably imatinib mesylate, with high polymorphic stability and the processes for the preparation thereof are disclosed.
US20100204191 Function-Selective Vitamin D Receptor Agonist The present invention provides a VDR ligand which does not induce hypercalcemia that is an adverse reaction of a vitamin D3 preparation; and a composition which comprises lithocholic acid propionate, a salt thereof, a solvate thereof, or a prodrug thereof.
US20090074792 Compositions containing full-length L1R nucleic acid and endoplasmic reticulum-targeting sequence, and methods of use The invention described here encompasses DNA and protein vaccines against poxviruses, and relevant immunogenic compositions, comprising at a minimum a nucleic acid encoding a modified full-length poxvirus L1R gene or its ortholog. The L1R gene is modified so that an endoplasmic reticulum-targeting sequence is operably linked on the 5′ end. Preferably the nucleic acid sequences for other poxviruses antigens are also included, such as A33R, B5R and/or A27L. These vaccines and compositions provide improved neutralizing antibody response elicited by molecular poxvirus vaccines, over known vaccines using unmodified L1R.
CN103373971A Urea compounds serving as protein kinase inhibitors The invention provides urea compounds serving as protein kinase inhibitors and medicinal salts of the urea compounds, as well as medicine compositions containing the compounds and application of the compounds as protein kinase inhibitors.
US20090074852 Lipoplex formulations for specific delivery to vascular endothelium The present invention is related to a lipid composition contained in and/or containing a carrier comprising at least a first lipid component, at least a first helper lipid, and a shielding compound which is optionally removable from the lipid composition under in vivo conditions, whereby the lipid composition containing carrier has an osmolarity of about 50 to 600 mosmole/kg, preferably about 250-350 mosmole/kg, and more preferably about 280 to 320 mosmole/kg, and/or whereby liposomes formed by the first lipid component and/or one or both of the helper lipid and the shielding compound in the carrier have a particle size of about 20 to 200 nm, preferably about 30 to 100 nm, and more preferably about 40 to 80 mm.
US7378419 3-{[(5,5a,8a,9)-9-(4-hydroxy-3,5-dimethoxyphenyl)-8-oxo-5,5a,6,8,8a,9-hexahydrofuro[3',4':6,7]naphtho[2,3-d][1,3]dioxol-5-yl]amino}-1-methyl-1H-pyrrole-2,5-dione; anticarcinogenic agent; inhibiting catalytic activity of topoisomerase II by stabilization of cleavable complex; better soluble and tolerated The invention relates to compounds of formula (I), wherein R1 is a group selected from hydrogen, alkyl, aryl, aryalkil, heteroaryl, heteroarylalkyl, alkylcarbonyl, arylcarbonyl, arylalkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, heterocycloalkoxycarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl, phosphonic and Si(Ra)2Rb, Y is a group selected from HN—NH and N—R2, R3 is a hydrogen atom, an alkyl, cycloalkyl, aryl, arylalkyl group, R4 is hydrogen atom or an alkyl group, enantiomers, diastereoisomers and the salts thereof
CN103446082A Application of salvianolic acid B to preparation of medicament for prevention and / or treatment of pulmonary microcirculation disorder or lung injury The invention provides application of salvianolic acid B to preparation of medicaments for prevention and / or treatment of pulmonary microcirculation disorder or lung injury. The invention discovers that salvianolic acid B can inhibit expression of pulmonary capilary endothelial cell adhesion molecule-1 and an E-selectin, inhibit adhesion of leucocyte in capillary vessels among alveolars, inhibit leakage of alhumin in capillary vessels among alveolars, inhibit concentrations of tumor necrosis factor alpha and interleukin-8 in blood plasma and alveolar irrigation solution, inhibit expression reduction of lung tissue aquaporin 1 and aquaporin 5, inhibit expression increase of lung tissue metalloprotease 2 and metalloprotease, and mitigate pulmonary edema and lung injury.
EP2240450A1 Trpa1 antagonists Compounds of formula (I), wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
WO2011002984A1 Substituted phenoxypropylcycloamine derivatives as histamine-3 (h3) receptor ligands The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
CN101422435A Tilmicosin liposome preparation and preparation method thereof The invention relates to a Tilmicosin lipidosome preparation and a preparation method. The Tilmicosin lipidosome preparation consists of the Tilmicosin lipidosome and the acceptable vector of a medicament; wherein, the Tilmicosin lipidosome contains Tilmicosin, phospholipid and cholesterin with the weight ratio of 1 : 2 to100 : 1 to 15; the acceptable vector of the medicament comprises an internal buffer system, alkali used for regulating pH, and a frozen-dried supporting agent; the adding amount of the frozen-dried supporting agent calculated according to the weight ratio of the phospholipid is as follows: 0.2 to 4 portions of the frozen-dried supporting agent is added into one portion of the phospholipid; the adding amount of the internal buffer system is 5 to 15mL. The invention has the advantages that: the Tilmicosin content in the unit volume of the Tilmicosin lipidosome preparation is high; the envelop rate is high; the stability is good; moreover, the medicament-loading rate is stable. The medicament in the lipidosome is continuously released, thus remarkably improving the concentration of blood medicament and prolonging the circulating time of the medicament in the blood. The Tilmicosin lipidosome preparation improves the curative effect of the medicament and enhances the clinic usability of the medicament.
EP1719526A2 Pharmaceutical combinations comprising a P2T receptor antagonist and another anti-thrombotic agent The present invention provides novel pharmaceutical combinations and their use in anti-thrombotic therapy.
US20090029955 Pyridothienopyrimidine Derivatives A pyridothienopyrimidine derivative of formula (I), or the pharmaceutically acceptable salts or N-oxides thereof are disclosed, as well as pharmaceutical compositions comprising said compounds and methods of treatment or prevention of a pathological condition or disease susceptible to amelioration by inhibition of phosphodiesterase 4 using said compounds are disclosed.
WO2010034670A2 Host cell kinases as targets for antiviral therapies against hcv infection The present invention provides several networks of cellular protein kinases as potential targets for medical intervention against hepatitis C virus (HCV) infection and HCV-related diseases and disorders in mammals, including humans. The invention relates to therapeutic protocols and pharmaceutical compositions designed to inhibit the activity of one or more of these protein kinases for the prevention and/or treatment of infections and diseases caused by HCV. The invention also relates to methods for the identification of kinase inhibitors that may be used to treat and/or prevent HCV infections and HCV-related diseases.
US20120269810 Methods and compositions for panic disorders Methods and compositions that down regulate the activity of orexins to treat panic disorder and panic-like responses associated with hypercapnic conditions are disclosed.
EP1469866B1 Cycloglycans suitable to inhibit mammalian infection The use of, in particular homopolymeric, cycloglycans with an annular base structure of 2 to 40 monosaccharides in the ring for the prevention of the invasion and infection of mammalian cells by pathogens. The treatment of diseases caused by said pathogens and foodstuffs and dietetic and pharmaceutical products comprising said cycloglycans.
WO2007098644A1 Benzopyran compounds and their preparation method and their usage The present application has disclosed benzopyran compounds of formula (I) and their pharmacologically acceptable inorganic salts or organic salts, in which the bond between 3- and 4- position can be a single bond or a double bond. When the said bond is a single bond, conformation of 4-carbon atom can be R or S or isomer and the substitutes are defined as description. The present application also provides the preparation method of such compounds and pharmaceutical compositions containing the compounds as active ingredient which are used to treat II type diabetes and its complication.
EP1712238A1 Anthracyclin induced immunogenic dead or dying cells composition The present invention is aimed at a composition comprising immunogenic dead or dying cancer cells or infected cells and fragments or fractions thereof obtained by treatment with anthracyclins, to a process of manufacturing said composition and to its use for treating cancer, for preparing a vaccine or for treating infectious diseases. It also relates to a medicament comprising at least one anthracyclin to be injected into or at the vicinity of the tumor.
CN102327615A Bone targeting vector and medicament The invention discloses a bone targeting medicinal vector and medicament. The bone targeting medicament vector is prepared by the following steps of: oxidizing glucan into glucan oxide containing a poly-aldehyde group with sodium periodate; and making diphosphonic acid containing an amino group react with the glucan oxide containing the poly-aldehyde group. The medicament with a bone targeting property is obtained by the following steps of: making the bone targeting medicament vector react with a medicament containing an amino group; and connecting the glucan oxide containing the poly-aldehyde group serving as an intermediate with diphosphonic acid with a bone guiding function and other medicaments (except diphosphonic acid) containing amino groups, wherein the prepared bone targeting medicament has high bone affinity and large medicament loading capacity when the reaction mass ratio of the diphosphonic acid to the glucan oxide aldehyde group is (0.4-0.6):1. The bone targeting medicament acts on bone tissues in an oriented way under the guiding action of the diphosphonic acid, and has different treating effects by loading different medicaments. The bone targeting medicament has the advantages of large medicament loading capacity, high bone affinity, simple synthesizing steps and easiness for controlling conditions.
US20100120918 Novel non-aqueous topical solution of diclofenac and process for preparing the same A non-aqueous topical solution composition of pharmaceutically acceptable salt of diclofenac is disclosed. The non-aqueous topical solution composition comprises therapeutically effective amount of pharmaceutically acceptable salt of diclofenac, solublizer, penetration enhancer and solvent, and optionally a humectant, counter irritant, additional penetration enhancer and anti-oxidants and a process for preparing the same.
CN103006956A Black ox horn oil-agent bonesetting paste The invention relates to a black ox horn oil-agent bonesetting paste which is characterized by immersing 200 grams of elderberry, 200 grams of sappan wood, 200 grams of dalbergia heartwood, 200 grams of nux vomica, 200 grams of achyranthes root, 200 grams of spatholobus stem, 200 grams of Pinus tabulaeformis, 200 grams of girald daphne bark, 130 grams of Datura stramonium, 120 grams of Chinese angelica, 160 grams of rhododendron molle, 16o grams of garden balsam stem, 120 grams of cortex acanthopanacis, 100 grams of safflower, 160 grams of clematis root and 100 grams of notopterygium root by using 10 kilograms of sesame oil, frying the above medicaments to a black carbon color, filtering to obtain medicinal oil, adding 240 grams of yellow lead into every 5 kilograms of the medicinal oil, heating the medicinal oil at a temperature of 320 to 360 DEG C till the medicinal oil changes from red to black, adding 340 grams of black ox horn, 200 grams of leather sheath, 100 grams of pseudo-ginseng, 160 grams of frankincense, 160 grams of myrrh and 100 grams of carbonized hair, and uniformly stirring into a plaster.
US7041311 Preparation for saliva flow The present invention is directed to products that promote saliva generation in the mouth through the use of various food grade acceptable acids. The products that enhance saliva production are preferably foods that are consumed in the mouth over a period of time of a minute or longer such as chewing gums, breath films, toothpaste and lozenges.
WO2013028909A1 Combination therapy for the treatment of sleep-related breathing disorders Provided herein are methods for treatment of sleep-related breathing disorders comprising administration of a dopamine-2 receptor antagonist and a sympathomimetic agent to an individual suffering from or suspected to be suffering from a sleep-related breathing disorder.
US8236774 Human telomerase catalytic subunit The invention provides compositions and methods related to human telomerase reverse transcriptase (hTRT), the catalytic protein subunit of human telomerase. The polynucleotides and polypeptides of the invention are useful for diagnosis, prognosis and treatment of human diseases, for changing the proliferative capacity of cells and organisms, and for identification and screening of compounds and treatments useful for treatment of diseases such as cancers.
WO2010021247A1 Pharmaceutical preparation, food or beverage having inhibitory activity on serotonin transporter Disclosed is a pharmaceutical preparation, food or beverage for treating or preventing a disease or condition which can be ameliorated through the inhibition of serotonin reuptake. The pharmaceutical preparation, food or beverage comprises a clinically effective amount of (1S,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3- carboxylic acid.
US20070270428 Use of Cyclooxygenase-2 Inhibitors for the Treatment of Depressive Disorders The invention concerns the use of compounds of formula (I), (II) and (III): which are COX-2 (cyclooxygenase-2) inhibitors, and pharmaceutically acceptable salts or solvates thereof, for the treatment of depressive disorders in combination with an effective amount of a second component which is a selective serotonin reuptake inhibitor.
EP1948176A1 Diaryl ureas for treating pulmonary hypertension The present invention relates to pharmaceutical compositions for treating, preventing or managing pulmonary hypertension comprising at least a diaryl urea compound optionally combined with at least one additional therapeutic agent. Useful combinations include e.g. BAY 43-9006 as a diaryl urea compound.
US20120329849 Unit dose formulations of ketorolac for intranasal administration This invention relates to therapeutic compositions, particularly sprayable aqueous compositions, and unit dose formulations comprise ketorolac or a pharmaceutically acceptable salt, alone or in combination with lidocaine or a pharmaceutically acceptable salt thereof. The compositions are nasally administered to a subject in need thereof to treat pain or inflammation.
US7250431 neuropeptide Y(NPY) receptor antagonists; useful in the treatment of obesity; such as 4-methoxy-N-{4-[5-(2-methyl-benzoyl)-thiazol-2-ylamino]-phenyl}-benzenesulfonamide Thiazole derivatives of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, a and b have the significance given in the specification. The compounds are neuropeptide Y Y5 receptor antagonists which can be used for the treatment of obesity.
EP2651948A1 Imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment hyperproliferative disorders The present invention relates to substituted imidazopyrazine compounds of general formula (I) : in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
EP1505960A1 Methods of treating gastrointestinal and genitourinary pain disorders using vinlafaxin and derivatives This invention provides a method of treating functional gastrointestinal and genitourinary disorders in a mammal by administering to the mammal an effective amount of hydroxycycloalkane phenethylamine of the following structural formula (I) in which A is a moiety of the formula (II) where the dotted line represents optional unsaturation; R1 is hydrogen or alkyl; R2 is alkyl; R4 is hydrogen, alkyl, formyl, or alkanol; R5 and R6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy; R7 is hydrogen or alkyl; and n is 0, 1, 2, 3, or 4, or a pharmaceutically acceptable salt thereof.
CA2808277A1 Novel colchicine derivatives, methods and uses thereof The invention relates to colchicine derivatives, methods and uses thereof for treatment of cancer. In certain embodiments, the colchicine derivative comprises a compound of formula (I), wherein Z is O or S; R1 is selected fro H, a halo group, a substituted or unsubstituted hydrocarbon group, or a substituted or unsubstituted heterogeneous group; R2 and R3 are each independently selected from H, a halo group, a substituted or unsubstituted hydrocarbon group, a substituted or unsubstituted heterogeneous group, a substituted or unsubstituted carbocyclic group, a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aromatic, or a substituted or unsubstituted heteroaromatic; R is selected from H or a substituted or unsubstituted hydrocarbon group, with the proviso that when R, R2 and R3 are methyl groups, R1 is not -COCH3.
CN102844431A Diacylglycerole acyltranferase gene, and use thereof Disclosed are a diacylglycerole acyltranferase, and a polynucleotide which codes for same. Provided are: a polynucleotide containing a base sequence represented by SEQ ID NO: 1 or 4; a polynucleotide which codes for a protein comprising an amino acid sequence represented by SEQ ID NO: 2; an expression vector and transformant containing said polynucleotide; a method for producing an aliphatic acid or a lipid using said transformant; and food containing the aliphatic acid or lipid which were produced by means of said method.
CN103463042A Application of Lycojaponicumin A in drugs for treating prostatic cancer The invention discloses application of Lycojaponicumin A in preparation of drugs for treating prostatic cancer and belongs to the technical field of new application of drugs. In vitro MTT anticancer activity evaluation discovers that Lycojaponicumin A shows remarkable inhibitory effects on growth of human prostatic cancer cell lines ALVA, gpc-1, 9L-B and Du145. Therefore, the Lycojaponicumin A can be used for preparing anti-prostatic cancer drugs and has good development and application prospects. Application of the Lycojaponicumin A in preparation of drugs for treating prostatic cancer is disclosed for the first time; and because skeleton type is completely new, inhibitory activity on prostatic cancer cells is extraordinary strong.
CN1850088A Pharmaceutical use of (2s-cis)-(+)-2,3-dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepine-4(5H)-one for treating hepatitis The present invention discloses a new application of (25-cis)-(+)-2.3-dihydro-3-hydroxy-2-(4-methoxphenyl)-1,5-benzothiazatropylidene-4-(5H)-ketone used as active component in preparation of medicine for effectively curing cocaine toxic hepatitis and carbon tetrachloride toxic hepatitis.
US20090291925 Bioactive polymeric liquid formulations of absorbable, segmented aliphatic polyurethane compositions Bioactive liquid formulations are formed of combinations of absorbable, segmented aliphatic polyurethane compositions and liquid polyether for use as vehicles for the controlled release of at least one active agent for the conventional and unconventional treatment of different forms of cancer and the management of at least one type of bacterial, fungal, and viral infection.
CN101151020B Adjuvanting material The present invention provides an adjuvanting material, the adjuvanting material comprising a lipid dendritic cell targeting moiety to which is covalently linked a metal chelating group. Further, the present invention provides an immunogenic composition comprising (a) a lipid dendritic cell targeting moiety to which is covalently linked a metal chelating group; (b) an antigen comprising a metal affinity tag; and optionally (c) metal ions, whereby the antigen is linked to the lipid dendritic cell targeting moiety via the interaction between the metal affinity tag and the metal chelating group.
WO2010047127A1 PHENANTHROINDOLIZIDINE COMPOUND AND NFκB INHIBITOR CONTAINING SAME AS ACTIVE INGREDIENT A novel compound having an excellent NFκB inhibitory effect. Specifically disclosed is a compound represented by formula (1) or a salt thereof. (In the formula, R1 represents a hydrogen atom, a lower alkyl group, a lower alkyloxy group or a halogen atom; R2 represents a hydroxy group or a lower alkyloxy group; R3 represents a hydrogen atom, a lower alkyl group or a halogen atom; R4 represents a hydrogen atom or a lower alkyloxy group; R5 represents a hydrogen atom, a lower alkyloxy group, a halogen atom or a hydroxy group, or alternatively forms a methylenedioxy group or an isopropylidenedioxy group together with R6; R6 represents a hydrogen atom or a lower alkyloxy group, or alternatively forms a methylenedioxy group or an isopropylidenedioxy group together with R5; R7 represents a hydrogen atom or a lower alkyl group; and R8 represents a hydrogen atom, a hydroxy group, an amino group or a lower alkylcarbonyloxy group (excluding the case wherein R1, R3, R4 and R7 are hydrogen atoms, R2 and R8 are hydroxy groups, and R5 and R6 are methoxy groups).)
CN101724041A Human epididymal expression sperm binding protein HEL-47 as well as encoding gene and application thereof The invention belongs to the biotechnology and the medical field and discloses a new human epididymal specific expression sperm binding protein HEL-47 as well as preparation and application thereof. The invention discloses an amino acid sequence of the HEL-47 protein and provides a recombinant expression vector which carries a DNA sequence used for encoding the protein. The protein is located in the neck region of a mature sperm, and an RT-PCR result indicates that the protein mainly has expression in an epididymis, a testis, a liver and tissues. A band of 47 KD is detected in the epididymis by using Western blot. The HEL-47 protein can be used as a target protein for developing an immunological contraceptive and clinically diagnosing and treating male infertility. A method for detecting a corresponding gene or protein based on development of the HEL-47 protein can be widely used for the research field of reproductive medicine.
CN1907979B 8-methylene-methylamine-5,7-dihydroxy-6,4'-dimethoxyisoflavone and medicinal composition with the same as active component The invention discloses a Nepal iris isoflavone derivant and drug salt with structure formula (I) and preparing method, which can improve or treat heart, chain vessel disease.
CN101219149A Auricularia polytricha polyoses grain medicinal granules and method for preparing the same The invention relates to instant granules of [Auricularia polytricha (Mont.) Sacc.] polysaccharide and a preparation method thereof, which is characterized in that: (by weight percentage) 5-10 percent of [Auricularia polytricha (Mont.) Sacc.] polysaccharide, 75-85 percent of sucrose powder and 10-25 percent of dextrin are well mixed and screened with a 60-mesh sieve to separate impurities and large granules; 1525 percent (by weight percentage) of the total obtained mixture is well mixed with 65 percent (by volume fraction) of edible alcohol, kneaded to form material like dough and vibrated, squeezed and screened with a 10-30 mesh sieve, and then dried at temperature of 60-65 DEG C for 2-4h to form granules, thus, the granules of [Auricularia polytricha (Mont.) Sacc.] polysaccharide are obtained via subpackage of the granules. The granules of [Auricularia polytricha (Mont.) Sacc.] polysaccharide of the invention are convenient for carrying and can be easily accepted. The [Auricularia polytricha (Mont.) Sacc.] polysaccharide extracted from the [Auricularia polytricha (Mont.) Sacc.] is similar to auricularia auricular polysaccharide, which is one of the six medicinal funguses with the strongest antineoplasmic activity.
CN102188484A Formula and manufacturing method of medicinal pad for thunder-fire moxibustion The invention relates to a formula and a manufacturing method of a medicinal pad for thunder-fire moxibustion. The preparation of the medicinal pad comprises the following steps: mixing frankincense, realgar, sulphur, camphor and borneol by a certain proportion; stirring uniformly; grinding the mixture into powder; putting the powder into a medicine bag; putting the medicine bag into a multilayer pad sewed in advance to finish the manufacture. The medicinal pad is an externally applied medicament without toxic effects, side effects or damages to organs. Raw material sources of the medicinal pad are wide, and a manufacturing method is simple and with low costs. Cooperated with moxibustion tools and externally applied pastes, the medicinal pad has substantial curative effects on scapulohumeral periarthritis, arthritis, cervical spondylosis, hyperosteogeny, herniated disk, ankylosing spondylitis, small area of leucoderma, asthma, chronic bronchitis, gastral cavity pain and diarrhea.
US20080038284 Human Immunodeficiency Virus Vaccine The present invention relates, in general, to human immunodeficiency virus (HIV) and, in particular, to an HLA-based HIV vaccine.
US20050043344 Such as 3-(3,5-ditert-butylphenyl)-4-{3-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl]-1,2,4-oxadiazol-5-yl}butanoic acid; for treatment of tumor metastasis, angiogenesis, osteoporosis, arthritis, retinopathy, smooth muscle cell migration, restenosis, and atheroscelorosis The present invention relates to pharmaceutical compositions comprising compounds of the Formula I, or a pharmaceutically acceptable salt thereof, and methods of selectively inhibiting or antagonizing the αVβ3 and/or the αVβ5 integrin without significantly inhibiting the αVβ6 integrin.
US8198329 Memory consolidation promoting agent and method of use A medicament for promoting memory consolidation, which comprises, as an active ingredient, a non-natural retinoid, preferably a retinoid having a basic skeleton comprising an aromatic ring bound with an aromatic carboxylic acid or tropolone by means of a bridging group, more preferably 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid or 4-[(3,5-bis-trimethylsilylphenyl)-carboxamido]benzoic acid.
US20120077818 Compositions comprising transnorsertraline and serotonin receptor 1a agonists/antagonists and uses thereof Provided herein are methods of and compositions for, treating, preventing and managing various neurological disorders. The methods comprise administering a transnorsertraline in combination with a serotonin receptor IA agonist, antagonist or modulator.
CN101912373A Stable cefeclor dispersible tablet and preparation method thereof The invention belongs to the technical field of medicament preparations, and particularly relates to a cefeclor dispersible tablet which is characterized by being prepared from the following components in parts by weight: 25g of cefeclor, 11.5g of microcrystalline cellulose, 5-7g of hydroxypropyl cellulose, a proper amount of 2-percent hydroxypropyl methylcellulose 40-percent ethanol solution, 5g of pregelatinized starch, 2.8-4g of cross-linked polyvidone, 1.2g of silicon dioxide, 1-2g of magnesium laurylsulfate and 0.12g of essence. Because the magnesium laurylsulfate is used in the dispersible tablet, the preparation stability is markedly improved, the content is basically not changed after long-time placement, and the service time of the medicament is prolonged.
US20100105755 Substituted benzamide modulators of dopamine receptor The present invention relates to new substituted benzamide modulators of dopamine receptor, pharmaceutical compositions thereof, and methods of use thereof.
US20110034450 Oxo-heterocyclic substituted carboxylic acid derivatives and the use thereof The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
CN103585124A Veterinary enrofloxacin chewable tablet The invention discloses a veterinary enrofloxacin chewable tablet which overcomes the defect of poor palatability of conventional tablets, can promote animals to chew completely for absorption, improves the veterinary disease curing rate, and reduces the medicine waste. The chewable tablet comprises the following components by weight percent: 1-5 percent of aspartame, 20-30 percent of oral glucose and skim milk powder mixture, 40-60 percent of excipient, 0.5-1 percent of glidant and 5-20 percent of enrofloxacin, wherein the ratio of the oral glucose to the skim milk powder in the mixture is (1:1) to (1:4).
US20120258986 Olefin containing nuclear transport modulators and uses thereof The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
WO2009029617A1 Diarylamine-substituted quinolones useful as inducible nitric oxide synthase inhibitors Novel diarylamine-substituted quinolone compounds and pharmaceutical compositions, certain of which have been found to inhibit inducible NOS synthase have been discovered, together with methods of synthesizing and using the compounds including methods for the treatment of iNOS-mediated diseases in a patient by administering the compounds.
WO2008152086A2 4,5-dihydro-(1h)-pyrazole derivatives as cannabinoid cb1 receptor modulators This invention relates to 4,5-dihydro-(1 H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions containing these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. The compounds have formula (I) wherein the symbols have the meanings given in the specification.
US20120052111 Adhesive Laminates for Rapid Wound Occlusion Provided herein are protective laminate devices comprising a biocompatible non-adherent substance and a fast-setting adhesive and methods of use. Also provided is a dispenser for an adhesive tape. The protective laminate devices and methods may be used for wound closure.
CN102240276A Granular preparation containing ambroxolhydrochloride and salbutamol sulfate and preparation method thereof The invention relates to a compound oral granular preparation containing ambroxolhydrochloride and salbutamol sulfate. 1,000 bags of the compound oral granular preparation consists of the following ingredients: 3.5 to 60 grams of ambroxolhydrochloride and 1 to 8 grams of salbutamol sulfate. A preparation method of the compound oral granular preparation comprises the following steps of: crushing and sieving the ambroxolhydrochloride and the salbutamol sulfate; sieving a diluted filling agent, a flavoring agent, an aromatic agent and a disintegrating agent; preparing an adhesive solution for later use; throwing materials according to the prescription; mixing the raw materials, the diluted filling agent, the flavoring agent, the disintegrating agent, the aromatic agent and the like uniformly; after adding an adhesive, extruding to prepare granules; performing forced air drying at the temperature of 50 DEG C; sieving the granules with the grain size of 180 to 2,000 mu m; and after detecting to be qualified, quantitatively subpackaging to prepare the compound oral granular preparation.
WO2009055644A3 Agonists and antagonists of guanylate cyclase receptors of the grueneberg ganglion for use in modulating animal behaviour The present invention relates to physical and pharmaceutical methods of increasing or decreasing the activity of the Grueneberg Ganglion (GG) in a subject. In one embodiment, the method comprising administering a compound to the GG, wherein the compound is an agonist or antagonist, respectively, for at least one guanylyl cyclase receptor or the receptor's downstream effectors. The present invention also relates to methods of screening candidate compounds for their ability to modulate the activity of the GG. The present invention also relates to methods and kits for positively identifying a GG neuron based upon the presence or absence of the pGC- G or pGC-A receptors.
US20080287475 4-(3-Aminopyrazole) Pyrimidine Derivatives for Use as Tyrosine Kinase Inhibitors in the Treatment of Cancer This invention relates to novel compounds having the formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
US20120129834 Serotonin receptor antagonists for use in the treatment of huntington's disease Methods are provided for the treatment and/or prophylaxis of Huntington's disease. In various embodiments the methods involve administration of one or more serotonin receptor antagonists. In certain embodiments the serotonin receptor antagonists include, but are not limited to loxapine, and/or a loxapine analogue, and/or cyproheptadine, and/or a cyproheptadine analogue (e.g., pizotifen).
CA2396865C Farnesyl protein transferase inhibitors for treating breast cancer The present invention relates to the use of farnesyl protein transferase inhibitors for preparing pharmaceutical com-positions for treating advanced breast cancer.
EP1699451B1 Use of silibinin together with alpha-liponic acid for the treatment of chronic obstructive pulmonary diseases The invention relates to the use of at least one effector of glutathione metabolism, together alpha liponic acid, the salts and/or prodrugs thereof for simultaneous or timed cytoprotective treatment of chronically obstructive lung diseases.
US8486400 Methods of inhibiting unwanted cell proliferation using an antibody that binds to sonic hedgehog and inhibits hedgehog signaling The present application is directed to compositions and methods for inhibiting angiogenesis and treating or preventing unwanted cell proliferation, including tumors, by inhibiting the hedgehog pathway, e.g., with an antagonist of the hedgehog pathway such as those disclosed herein.
CN103040755A APARPAR polypeptide-modified invisible liposome and drug delivery system The invention discloses an APARPAR polypeptide-modified invisible liposome and a drug delivery system. The APARPAR polypeptide is modified on the surface of an invisible liposome. The membrane of the invisible liposome contains hydrogenated soybean lecithin, cholesterol, polyethylene glycol-stearoyl phosphatidyl ethanolamine and tearoyl phosphatidyl ethanolamine-polyethylene glycol-APARPAR. The invention further relates to the drug delivery system. The drug delivery system is formed by encapsulating an anti-tumor drug encapsulated with the APARPAR polypeptide-modified invisible liposome. The liposome drug delivery system can be used for targeted therapy of glioma and can go through the walls of blood vessels in a tumor mass under the mediating action of the APARPAR polypeptide to penetrate the inside of the whole tumor mass, so that the effect of killing the tumor cells is greatly improved.
EP1009440B1 Method for inhibiting immunostimulatory dna associated responses The invention features methods for inhibiting immunostimulatory DNA-associated immune responses, through the administration of specific compounds of the general class of 9-aminoacridines and 4-aminoquinolines. The invention also features methods of screening compounds useful in inhibiting immunostimulatory DNA-induced immune responses.
CN101606985A Liniment for treating sheep infective pustule virus and preparation method thereof The invention provides a liniment for treating sheep infective pustule virus and a preparation method thereof and relates to a medicine for treating infective pustule virus and a preparation method thereof. The invention overcomes the defects of slow effect taking, poor curative effect, inconvenient use and use restriction existing in the existing medicine for treating the sheep infective pustule virus. The liniment for treating the sheep infective pustule virus is prepared from red tall grass, isatis leaf, matrine n-oxide, Tween-80, benzyl alcohol and glycerol. The preparation method of the liniment is carried out according to the following steps: (1) weighing raw materials; (2) extracting the effective components of the red tall grass and the isatis leaf; (3) regulating the pH value and further extracting the effective components; (4) adding the matrine n-oxide, the Tween-80, the benzyl alcohol and the glycerol and sterilizing; and finally, obtaining the liniment for treating sheep infective pustule virus. The liniment for treating sheep infective pustule virus has the advantages of fast effect taking, high cure rate, convenient use and no restriction.
CA2675979A1 Treatment of cancers having resistance to chemotherapeutic agents The present invention provides compositions and uses thereof for treating cancer with DAST, 4 {4- [3- (4-chloro-3-trif luoromethyl phenyl) -ureido] -3 -fluorophenoxy} -pyridine-2-carboxylic acid methylamide of the formula I, including all polymorphs, hydrates, pharmaceutically acceptable salts, metabolites, prodrugs, solvates or combinations thereof. Any cancer can be treated, including cancers that have acquired resistance to another therapeutic agent, such as kinase inhibitors. DAST can also be used to treat cancers which have become refractory to other chemotherapeutic agents.
WO2011058193A1 [1,5]-diazocin derivatives The present invention relates to compounds of formula (I) compositions, in particular pharmaceutical compositions, and medicaments comprising at least one compound of formula (I). The invention also relates to the use of such a compound for manufacturing a medicament. In particular the medicament and the pharmaceutical composition are intended to treat diseases linked with insulin regulation problems, such as diabetes. This invention aims also to methods for treating or preventing such diseases.
WO2009021750A3 Benzoxazole, benzimidazole and benzothiazole derivatives and their use in the treatment of duchenne muscular dytrophy There are disclosed compounds of Formula (1). Pharmaceutical compositions containing the compounds are also provided. Methods of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy and cachexia using the compounds and compositions are also provided.
WO2009128050A3 An histone deacetylase inhibitor in combination with a sirtuin activator agent for the treatment of neurodegenerativediseases and tumors or neoplasms The present invention relates to a pharmaceutical composition comprising at least one histone deacetylase inhibitor, and at least one sirtuin activator agent having the general formula described. Such composition is used as a medication to treat chronic neurodegenerative diseases, and/or in the treatment of tumours or neoplasms.
CN101836983A Lansoprazole-containing pharmaceutical preparation and preparation method thereof The invention relates to a lansoprazole-containing pharmaceutical preparation and a preparation method thereof. Lansoprazole as a main active ingredient and pharmaceutical acceptable excipients are made into the preparation by a certain process, wherein the unit preparation content of the lansoprazole is 10-40mg, and is preferentially 15-30mg.
US20120328563 Cd4+cd25+ regulatory t cells from human blood The present invention provides suppressive and/or regulative human CD4+CD25+ T cells, a method for expanding same, and the use of the suppressive and/or regulative human CD4+CD25+ T cells and the expanded T cells as regulatory agent.
CN101062045B Use of triterpene saponin compounds in preparing tumor medicine The invention relates to the pharmaceutical use of triterpenoid saponin compounds, in particular to the novel use in preparing anti-tumor medicaments. The triterpenoid saponins compounds have appreciable actions of suppressing multiple tumor cells such as human gastric cancer cell lines and leukemia cell lines. Using these compounds as active constituents independently or in combination with other medicaments, anti-tumor drugs can be prepared.
WO2010090300A1 Diazepinedione derivatives Diazepinedione derivatives represented by general formula (I) or pharmacologically acceptable salts thereof are used as P2X4 receptor antagonist. In general formula (I), R1 represents a hydrogen atom, a C1-8 alkyl group, or the like; R2 represents a hydrogen atom, a C1-8 alkyl group, a C1-8 alkoxy group, a mono-, di-, or tri-halogenated C1-8 alkyl group, a halogen atom, a hydroxyl group, a nitro group, an amino group, a carboxyl group, a cyano group, or the like; R3 represents a hydrogen atom, a C1-8 alkyl group, or the like; and R4 and R5 may be the same or different and each represents a hydrogen atom, a C1-8 alkyl group, or the like.
US7262180 For therapy of dermatitis conditions and skin impairments such as atopic dermatitis, contact dermatitis, allergic contact dermatitis, allergic dermatitis, seborrheic dermatitis, nummular dermatitis, chronic dermatitis of hands or feet, generalized exfoliative dermatitis, stasis dermatitis The present invention relates to compositions comprising telmesteine, glycyrrhetinic acid, and a proanthocyanidin, as well as methods for using such compositions in the treatment of an inflammatory condition of the skin including, but not limited to, atopic dermatitis(eczema), allergic contact dermatitis, seborrheic dermatitis, psoriasis, xerosis and atopia, as well as treatment of an inflammatory condition of mucosae and of an inflammatory condition in the eye. The present invention also relates to compositions comprising a proanthocyanidin, glycyrrhetinic acid and telmesteine, as well as methods for using such compositions in the treatment of an inflammatory condition of the skin including, but not limited to, atopic dermatitis, allergic contact dermatitis, seborrheic dermatitis, radiation dermatitis, psoriasis, xerosis and atopia, as well as treatment of an inflammatory condition of mucosae and of an inflammatory condition in the eye.
CN103301136A Combined medical and health-care medicine of naringenin The invention provides an application of natural brassinolide analogues and naringenin in preparation of medicines for preventing or treating mammal diseases (in particular male mammals), or an application in preparation of health-care products for health-care of mammals. In addition, the invention further provides a corresponding medicine or health-care composition and a preparation method thereof.
WO2010140092A1 L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
EP1028729B1 Methods of modulating serine/threonine protein kinase function with 5-azaquinoxaline-based compounds The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with 5-azaquinoxaline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to 5-azaquinoxaline compounds and pharmaceutical compositions comprising these compounds.
US20100048506 Composition for treating arthritic disorder The present invention provides compositions and methods for treating a joint disease containing as an active ingredient thereof a monovalent metal salt of alginic acid for which the endotoxin level thereof has been lowered to an extent that does not substantially induce inflammation or fever. As a result, it is possible to provide a composition for treating a joint disease which has the effects of protecting cartilage from mechanical irritation, inhibiting degenerative changes in cartilage caused by wear and inflammation, repairing cartilage injuries, suppressing inflammation and pain of joint tissue, inhibiting degeneration of synovial tissue, and inhibiting osteochondral destruction.
CN1765884A Antimycotic compound and its preparation method and uses The invention discloses an antimycotics compound with name as bis (4-fluorophenyl)methyl 2-(1-pyrrolidinyl)ethyl ether, as well as its preparation method, drug composition and application for infectious diseases.
CN102120751A Nucleoside compound with anti-cancer and anti-virus activities, and preparation method and application thereof The invention discloses a nucleoside compound with anti-cancer and anti-virus activities, and a preparation method and application thereof, relates to the technical field of medicaments, in particular to a series of new nucleoside compounds with anti-cancer and anti-virus activities, and a preparation method and application thereof. The invention relates to a series of new nucleoside compounds with the structure of a formula (I) and the anti-cancer and anti-virus activities. The invention also relates to a preparation method of the nucleoside compounds with the structure of the formula (I). The nucleoside compounds with the structure of the formula (I) is prepared from xylose derivatives serving as raw materials through multi-step reactions. The nucleoside compounds have activities of resisting tumor cells and hepatitis B virus and have potential application to preparation of medicaments for resisting tumor and hepatitis B diseases.
CA2462510C Wipe formulation The present invention relates to a liquid formulation for a feminine wipe. The preferred formulation has an anti-irritant agent, a pH adjuster namely citric acid, and at least one preservative.
US20090275630 Cosmetic composition comprising an imidopercarboxylic acid derivative and a n-acylated amino acid ester Composition containing, in a physiologically acceptable medium, at least one imidopercarboxylic acid compound and at least one N-acylated amino acid ester of formula (A) as described herein.
CN103393702A Drug composition for enhancing memory of people rapidly exposed to high altitude, and preparation method thereof The present invention discloses a drug composition for enhancing memory of people rapidly exposed to a high altitude. The drug composition comprises an active component and an auxiliary material, wherein the active component comprises taurine, ovolecithin, acetyl-L-carnitine, and huperzine a, and the auxiliary material comprises lactose, MCC and magnesium stearate, or comprises lactose and magnesium stearate. The drug composition has the following beneficial effects that: based on different mechanisms such as provision of essential nutrients for nerve cells, free radical removing, neurotransmitter acetylcholine precursor complementing, central cholinergic system regulation, and the like, a comprehensive effect is acted on human body, drug combination advantages are presented, and improvement of memory of people rapidly exposed to a high altitude is achieved.
CN102964308A Novel pyrimidine compound, preparation method thereof, pharmaceutical composition containing novel pyrimidine compound and application of novel pyrimidine compound The invention relates to pyrimidine derivate as shown in a formula I, and pharmaceutically acceptable salt, hydrate, solvate and prodrug of the pyrimidine derivate. The invention also relates to a compound which is shown in the formula 1 and has high inhibitive capability to c-Met kinase, and relates to a compound and pharmaceutically acceptable salt and hydrate thereof, a preparation method of the compound, a pharmaceutical composition containing the compound, and application of the compound.
WO2008024930A2 Intrathecal administration of triptan compositions to treat non-migraine pain Intrathecal delivery of a pharmaceutically acceptable formulation for intrathecal administration of any drug selectively binding to this receptor to provide pain can be used in any situation in which intrathecal ('IT') drugs are presently used for pain management. In the preferred embodiment, the drug is a triptan. In another embodiment, a combination of drugs with triptans can be used instead of just the triptan. Exemplary conditions to be treated include cancer pain, chronic back pain, post-herpetic neuralgia, and complex regional pain syndrome types I or II, as well as post-traumatic pain, diabetic vasculopathy, inflammatory radiculopathy, inflammatory plexopathies such as brachial plexopathy (Parsonage Turner syndrome), or lumbar plexopathy, HIV neuropathy, chemotherapy-induced neuropathy (such as vincristine toxicity), erythromelalgia, and inherited painful disorders such as metachromatic leukodystrophy, Friedreich's ataxia, and Fabry's disease. The triptans can also be used in acute pain management, such as in labor management or spinal blockade for surgery, where a spinal formulation of sumatriptan could be combined with traditional opiates for synergistic or additive effects.
US20110166164 THIAZOLO[5,4-d] PYRIMIDINES AND THEIR USE AS AGROCHEMICALS The present disclosure relates to thiazolo[5,4-d]pyrimidines and their use as agrochemicals and animal health products.
CN101475574B Camptothecin derivative, and preparation and use thereof The invention provides camptothecine compounds of a formula (I) and the pharmaceutically acceptable salts of the same and also relates to methods for preparing the same, pharmaceutical compositions containing the same and the uses and intermediates of the same.
CN101347412A Amifostine trihydrate crystal lyophilized preparation and method of preparing the same The invention belongs to the field of pharmaceutical preparations and discloses a sterile lyophilized crystalline amifostine trihydrate preparation and a preparation method thereof. The sterile lyophilized crystalline amifostine trihydrate preparation is prepared by the mixed solution consisting of the mixing solvent of amifostine, acetone, ethanol and water after the steps of removing pyrogen, filtering and sterilizing by a 0.22mum membrane, filling, pre-freezing, lyophilizing, sublimation and analysis drying, aerating and stopper pressing. The lyophilized crystalline amifostine trihydrate preparation has the advantages of stable performance, convenient preparation process, short process time with the lyophilization process time less than 35 hours, energy saving, high efficiency, being suitable for large-scale production and being easy for transport and storage.
CN103536589A Preparation method of compound nano lipidosome capable of improving bioavailability of catechinic acid The invention discloses a preparation method of compound nano lipidosome capable of improving the bioavailability of catechin. The method comprises the following steps: 1) adding 100mg to 150mg of catechin and 1.0g to 2.0g of tween80 into 20ml of 0.05mol/L phosphate buffer (PBS, pH7.0) so as to obtain a mixture, and stirring the mixture at the temperature of 40-60 DEG C to obtain a catechin PBS solution; 2) weighing and dissolving 100mg to 200mg of probenecid, 0.1g to 0.5g of lecithin and 100mg to 500mg of cholesterol in 10ml to 20ml of dichloromethane so as to obtain a mixture I, injecting the mixture I into the catechin PBS solution obtained in step 1) by utilizing a syringe at the temperature of 40-60 DEG C so as to obtain a mixture II, and stirring the mixture II at a constant temperature to obtain a suspension; 3) evaporating the suspension in a rotating state to remove the dichloromethane; carrying out the ultrasonic treatment on the mixture by utilizing the ultrasonic of 350W to 400W for 8min to 12min to obtain the catechin compound nano lipidosome.
CN102302490A Medicine composition of imipenem-cilastatin-tazobactam The invention provides a combination medicine, and specifically provides a combination medicine of imipenem-cilastatin-tazobactam for treating infectious diseases caused by acinetobacter baumanii. The combination medicine of imipenem-cilastatin-tazobactam has synergistic and accumulated antibacterial effects on the infectious diseases caused by acinetobacter baumanii, particularly has excellent synergistic and accumulated antibacterial effects on a multidrug-resistant acinetobacter baumanii strain, and also can be used for curing clinical infection caused by the multidrug-resistant acinetobacter baumanii.
US20050020540 Biphenylcarboxylic amide derivatives as p38-kinase inhibitors Compounds of formula (I): or pharmaceutically acceptable sats or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
CN1629128A Method for preparing leucogen materials and leucogen tablets The invention discloses a method for preparing leucogen materials and leucogen tablets for treating thrombocytopenia and regenerative anemia, which consists of, subjecting ethyl phenylacetate, ethyl formate, ethyl ether, metallic sodium to condensation, acidifying, and cyclization to obtain the leucogen raw material, thus subjecting the leucogen raw powder, dextrin, starch, cane sugar powder, ethanol (60%) and magnesium stearate to sieving, mixing, palletizing, and stamping.
WO2005077355A1 Pharmaceutical compositions for the prevention or treatment of diseases accompanied by esophageal dyskinesia Pharmaceutical compositions containing as the active ingredient aminoethylphenoxyacetic acid derivatives represented by the general formula (I) or pharmacologically acceptable salts thereof which are useful in the prevention or treatment of diseases accompanied by esophageal dyskinesia such as achalasia of esophagus, esophagism, or dysphagia: wherein R1 is hydrogen, lower alkyl, or aralkyl; R2 is hydrogen or halogeno; and carbon with (R) affixed thereto takes R-configuration, while carbon with (S) affixed thereto takes S-configuration.
CN101224216A Medicine compounds for anti-tumor The invention pertains to the bio-pharmaceutical field and relates to a medicine combination for treating tumor. The tumor is the worldwide No. 2 killer of human being and the drug resistance is one of the difficulties in the treatment of the tumor diseases. Therefore, to find a chemical compound which can reduce drug resistance is one of the hot topics in the study field of tumor disease. The invention provides the medicine combination for treating tumor and the medicine combination comprises nucleic acid with a gene sequence of 5'-GCCAGUGGAGGCUUCCAGG-3' or 5'-GCCAGTGGAGGCTTCCAGG-3' and daunomycin. The application of the nucleic acid and the daunomycin can dramatically reduce the drug resistance of tumor cells.
US20090093493 1-phenylalcoxy-2-beta-phenylethyl derivatives as p-glycoprotein (p-gp) inhibitors useful in drug resistance events The invention relates to a new class of compounds, which are 1-phenylalcoxy-2-β-phenylethyl derivatives, as P-glycoprotein (P-GP) inhibitors. These compounds are useful in drug resistance events. They have been shown able to inhibit in a dose-dependent manner Glycoprotein-P (P-gp) activity in cell lines in which the expression of said glycoprotein is very high, like Caco-2 (human colon cancer) cells and MCF7/Adr (adriamycin-resistant human breast carcinoma) cells. The invention also relates to methods of production and the utilization of such compounds as medicaments useful in the treatment of states linked to the difficulty for some drugs to cross the blood-brain barrier (BBB) and generally within the context of the problems of drug resistance induced by chemotherapy agents.
WO2009052126A1 PIPERIDINYL AND PIPERAZINYL MODULATORS OF γ-SECRETASE The present invention relates to compounds of Formula (I) as shown below, wherein the definitions of Het, R0, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula (I) are useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer´s disease.
US7678786 Benzoazepin-oxy-acetic acid derivatives as PPAR-delta agonists used for the increase of HDL-C, lower LDL-C and lower cholesterol The invention is directed to compounds of Formula (I) useful as PPAR agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, diabetes, nephropathy, neuropathy, retinopathy, polycystic ovary syndrome, hypertension, ischemia, stroke, irritable bowel disorder, inflammation, cataract, cardiovascular diseases, Metabolic X Syndrome, hyper-LDL-cholesterolemia, dyslipidemia (including hypertriglyceridemia, hypercholesterolemia, mixed hyperlipidemia, and hypo-HDL-cholesterolemia), atherosclerosis, obesity, and other disorders related to lipid metabolism and energy homeostasis complications thereof, using compounds of the invention are also described.
US20070161646 Piperidine Derivatives and Their Use as Modulators of Chemokine Receptor Activity (Especially CCR5) Compounds of formula (I): wherein L is CH or N; M is CH or N; provided that L and M are not both CH; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
CN102600117A Application and preparation method of ambroxol hydrochloride in preparation of information therapeutic drug and novel drug prepared by preparation method The invention discloses application of ambroxol hydrochloride in the preparation of an information therapeutic drug, a preparation method of the ambroxol hydrochloride and a novel drug prepared by the preparation method. The information treatment drug is characterized in that the drug does not contact a human body directly in the treatment, any substance ingredient of the drug can not be consumed, only the drug information is utilized for physical treatment, but the chemical treatment effect can be achieved, a treatment window is enlarged by more than 1000 times, and the side effects of the chemical treatment are avoided. After the ambroxol hydrochloride is used as the information treatment drug, the contents of active ingredients are not changed, and the ambroxol hydrochloride can be used as the conventional preparation in the chemical treatment for secondary effective use.
CN1596886A Application of albi multisulfoxide and its salt in preparing medicine for preventing and treating respiratory tract virus infestation An application of Albiduoya sulfoxide and its biocompatible salts in preparing the medicines for preventing and treating the virus infection of respiratory tract, such as viral influenza, is disclosed.
US20080051327 Crystals of an Aurora-A Tpx2 Complex, Tpx2 Binding Site of Aurora-A, Aurora-A Ligands and Their Use The present invention relates to crystals of phosphorylated Aurora-A kinase fragment alone and in complex with a ligand, amino acid residues 1-43 of human TPX2. This invention also relates to methods for designing and selecting ligands, in particular allosteric inhibitors of Aurora-A, that bind to the Aurora-A kinase and their use. Further, the present invention relates to certain indene and indole derivatives. The present invention relates to crystals of phosphorylated Aurora-A kinase alone and in complex with a ligand, amino acid residues 1-43 of human TPX2. This invention also relates to methods for designing and selecting ligands that bind to the Aurora-A kinase and their use. Further, the present invention relates to certain indene and indole derivative.
WO2010054253A1 Triazine derivatives as inhibitors of phosphodiesterases The invention relates to triazine derivatives of formula (I): which are inhibitors of phosphodiesterase 2 or 10, useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.
EP2402325A2 Hydroxylated and methoxylated cyclopenta[d]pyrimidines as AKT protein kinase inhibitors The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer. Further provided are method of synthesis of these compounds and intermediates in the synthesis process.
US7504386 comprised of benzyl esters of hyaluronic acid and/or internally cross-linked derivatives of hyaluronic acid and may be in the form of gels, membranes, woven tissues or meshes and nonwoven tissues; adhesion prevention New biomaterials essentially constituted by esterified derivatives of hyaluronic acid or by cross-linked derivatives of hyaluronic acid for use in the surgical sector, particularly for use in the prevention of post-surgical adhesions.
US20110039788 Compositions, methods and kits for detecting and treating cancer Compositions, kits and methods for inhibiting cancer cell (e.g., breast cancer cell) growth and treating a subject with cancer (e.g., breast cancer) include a therapeutically effective amount of an LBH inhibitor for inhibiting cancer cell growth and a pharmaceutically acceptable carrier, and/or a therapeutically effective amount of Wnt7a protein or nucleic acids encoding Wnt7a protein for inhibiting cancer cell growth and a pharmaceutically acceptable carrier. Methods of treating a subject having cancer (e.g., estrogen receptor negative basal-type breast cancer) include administering to the subject a composition including a pharmaceutical carrier and at least one of: an LBH inhibitor, a WNT7a protein, and a nucleic acid encoding WNT7a protein in an amount effective for inhibiting growth of cancer cells in the subject. Methods of detecting the presence of cancer (e.g., estrogen receptor negative basal-type breast cancer) in a subject include obtaining a biological sample from the subject; contacting the sample with at least one reagent that detects presence of LBH expression; measuring the level of LBH expression in the biological sample; and correlating overexpression of LBH with the presence of cancer (e.g., estrogen receptor negative basal-type breast cancer) in the subject. Kits for detecting the presence of basal-type breast cancer in a subject include at least one reagent for detecting the presence of LBH expression in a biological sample from the subject and instructions for use.
US7317014 pyrimidine derivatives such as 4-Chloro-5,6-diphenyl-2-(trifluoromethyl)pyrimidine, used for the treatment of inflammation and immunological diseases The present invention relates to novel derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel pyrimidine derivatives of the general formula (I)
US7015228 4-amino-2-(2-pyridyl)pyrimidines as microbicidal active substances Compounds of formula wherein R1 and R2 are each independently of the other hydrogen; unsubstituted or mono- or poly-halo-substituted C1–C20alkyl, C1–C20alkoxy, C2–C20alkenyl, C2–C20alkynyl, C3–C18cycloalkyl, C3–C7cycloalkyl-C1–C20alkyl; hydroxy; C1–C6alkoxy-C1–C20alkyl; carboxy; C1–C6alkyloxycarbonyl; cyano; mono- or di-C1–C20alkylamino; C1–C6alkylamino-C1–C20alkyl; halogen; phenyl; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted phenyl-C1–C20alkyl, phenoxy or phenyl-C1–C20alkoxy; or R1 and R2 form a polymethylene chain of formula —(CH2)m— wherein m=2–12; R3 is unsubstituted C7–C20alkyl; or amino-, hydroxy-, carboxy- or C1–C6alkyloxycarbonyl-substituted C2–C20alkyl; C8–C18cycloalkyl; C8–C20alkenyl; C8–C20alkynyl; C3–C7cycloalkyl-C8–C20alkyl; C1–C4alkoxy-C8–C20alkyl; R7R8N—C7–C20alkyl; phenyl; phenyl-C1–C4alkyl; or phenyl-C1–C4alkoxy; R4 is hydrogen; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted C1–C20alkyl, C2–C20alkenyl, C2–C20alkynyl, C3–C20cycloalkyl, C3–C7cycloalkyl-C1–C20alkyl, C1–C20alkoxy-C1–C6alkyl or R7R8N—C1–C20alkyl, phenyl, phenyl-C1–C20alkyl or phenoxy-C1–C20alkyl; R5 and R6 are each independently of the other hydrogen; C1–C20alkyl; C2–C20alkenyl; C2–C20-alkynyl; C3–C18cycloalkyl; C3–C7cycloalkyl-C1–C20alkyl; hydroxy; C2–C20alkoxy; C1–C6alkoxy-C1–C20alkyl; carboxy; C1–C6alkyloxycarbonyl; cyano; nitro; C1–C20alkylamino; C1–C20alkylaminoalkyl; C1–C20haloalkyl; C1–C20haloalkoxy; halogen; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted phenyl, phenoxy or phenyl-C1–C20alkyl or phenyl-C1–C20alkoxy; or R5 and R6 together form a polymethylene chain of formula —(CH2)m— wherein m=2–12; and R7 and R8 are each independently of the other hydrogen; C1–C20alkyl; C3–C20alkenyl; C3–C20alkynyl; C3–C7cycloalkyl; C3–C20cycloalkyl-C1–C4alkyl; phenyl; or phenyl-C1–C4alkyl are suitable for the antimicrobial treatment of surfaces.
EP2785720A1 Heterocyclic amides compounds which are hdac6 inhibitors and used as anti-tumoral agents The present document describes compounds of Formula I, pharmaceutical compositions comprising the same as well as methods of treating diseases such as a cancer, neurological disease, neurodegenerative disorder, stroke, traumatic brain injury, parasitic infection, inflammation or an autoimmune disease with said compounds.
CN101709058A Polyene macrolides compound, preparation and application thereof The invention provides a new compound having medicinal value, a preparation method thereof and a new bacterial strain which can generate the compound. The compound with formula (I) is chosen and prepared by rapidly choosing bacillus from soil sample with specific primer, using 16Ss rRNA gene to preliminarily identify and separate bacterial strain, amplifying, sequencing and comparing partial sequence of NRPSs/PKSs gene cluster after choosing potential new resources, analyzing the diversity of metabolite thereof, acquiring bacterial strain F6-B70 which contains new NRPSs/PKSs gene cluster and has new potential after choosing a large amount, fermenting in a fermentation medium, extracting active substance from bacterial cell and fermenting liquid, and then separating and purifying by using multiple purification techniques. The compound is a polyene macrolides compound which has an obvious function of restraining drug-resisting staphylococcus and an activity of resisting tumor.
US7122547 Anthranilic acid amides and the use thereof as medicaments The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.
US20120245208 2-Oxo-1-Pyrrolidinyl Imidazothiadiazole Derivatives The present invention relates to 2-oxo-1-pyrrolidine imidazothiadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
WO2012116010A3 Antibiotic tolerance inhibitors The present disclosure relates to benzimidazole-benzamide derivatives, and the use thereof, e.g., to treat infections.
WO2013129970A3 Pharmaceutical composition having vasoconstricting, anticongestant and anti-inflammatory activity (embodiments) The invention relates to the field of the pharmaceutical industry and medicine and can be used for the production and application of pharmaceutical compositions having vasoconstricting, anticongestant and anti-inflammatory activity in cases of acute rhinitis, inflammatory processes of the maxillary sinuses, nosebleeds and conjunctivitis. The problem of the invention consists in producing a pharmaceutical composition on the basis of the preparation naphazoline by introducing mineral substances into the pharmaceutical composition, and substituting 12С carbon isotopes with 13С carbon isotopes in the pharmaceutical composition.
US20100119570 Solid Pharmaceutical And Vaccine Dose An elongate body for parenteral injection at low velocity from a device is described. The body has at least one pointed end and comprises at least one active material. In addition, the body has a compressive strength of greater than or equal to 5 Newton and the pointed end has an included angle of between about 10-50°. A solid vaccine formulation for needle-free parenteral delivery, methods for making the body, packaging of the body and use of the body, packaging and suitable delivery device are also described.
US20100284916 Antibodies Against Human Cytomegalovirus (HCMV) The present invention provides novel antibody sequences that bind human cytomegalovirus (hCMV) and neutralize hCMV infection. The novel sequences can be used for the medical management of hCMV infections, in particular for preparing pharmaceutical compositions to be used in the prophylactic or therapeutic treatment of hCMV infections.
CN103732265A Anti-adhesion medical material and method for producing same Provided is an anti-adhesion medical material in which a polyhydric alcohol or a polyhydric alcohol aqueous solution containing a polyhydric alcohol is retained in a bioabsorbable base material that contains a bioabsorbable material and has a degree of swelling of 200 to 3,000 mass% and a water elution rate of 10 mass% or lower, and in which the residual amount of polyhydric alcohol after three hours of immersion in 25 DEG C water 50 or more times the total mass of the polyhydric alcohol aqueous solution or the polyhydric alcohol aqueous solution and the bioabsorbable base material is 30 mass% or less of the amount of polyhydric alcohol prior to immersion.
CN102920684A Tetradotoxin mask and preparation method thereof The invention discloses a tetradotoxin mask and a preparation method of the mask. The tetradotoxin mask comprises an active pharmaceutical ingredient tetradotoxin, stabilizer lactose, a complex solubilizer citric acid, zinc oxide, rosin, vaseline and mint essential oil and the like. Based on different amounts of tetradotoxin contained in the mask, the mask has the effects of relieving itching, easing pain and lifting face. The tetradotoxin mask changes the traditional administration manner of tetradotoxin, and is more convenient to use. The tetradotoxin mask is low in price, simple and easy to manufacture, fast in effect, long in lasting time, healthy and clean. In addition, the mask further conquers the social safety hazard caused by the original tetradotoxin injection is missed, and facilitates promoting normalization of the face lifting item. The consumer can quickly, conveniently and comfortably care the skins without beautifying medical institutions.
USRE39199 Antipsoriatic compositions, method of making, and method of using A psoriasis treatment composition derived from the plant Asphodelus Microcarpus includes 3-methylanthralin, chrysophanol, aloe-emodin, aloe-emodin monoacetate, and/or derivatives thereof. The composition is prepared by extracting a liquid from the Asphodelus Microcarpus root and mixing the liquid with acetic acid. A method of treatment includes applying the composition to an affected area of skin at a frequency sufficient to effect an alleviation of symptoms, typically once per day for 14-56 days.
EP2300437B1 Benzpyrazol derivatives as inhibitors of pi3 kinases The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
EP1726592A1 Dioxino derivatives and their use as dopanine agonists The compounds of formula I wherein R1 and R2 are, independently, hydrogen, alkyl, phenyl pr benzyl; or R1 and R2, taken together, are benzylidene optionally substituted with R3 as defined below or alkylidene, or R1 and R2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, arylalkoxy, alkanoyloxy, amino, mono-or di-alkylamino, alkanamido or alkanesulfonamido; R4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclic alkyl, phenyl optionally substituted with R3 as defined above, phenoxy optionally substituted with R3 as defined above, naphthyl optionally substituted with R3 as defined above or naphthyloxy optionally substituted with R3 as defined above, heteroaryl or heteroaryloxy, in which the heterocyclic ring of the heteroaryl or heteroaryloxy group is selected from thiophene, furan, pyridine, pyrazine, pyrimidine, indole, indazole, imidazole, chroman, coumarin, carbostyril, quinoline, benzisoxazole, benzoxazole, pyrazole, pyrrole, thiazole, oxazole, or isoxazole and the heterocyclic ring is optionally substituted by R3 as defined above; or a pharmaceutically acceptable salt thereof, are useful in treating disorders of the dopaminergic
CA2672661A1 Process for the preparation of piperazinyl and diazepanyl benzamide derivatives The present invention is directed to a novel process for the preparation of piperazinyl and diazapanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
CA2402300C Fluorocarbon aerosol medicaments This invention relates to aerosol formulations of use for the administration of medicaments by inhalation, in particular a pharmaceutical aerosol formulation which comprises particulate medicament selected from the group comprising salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate and physiologically acceptable salts and solvates thereof and a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, which formulation is substantially free of surfactant. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as defined is also described.
CN101134745A Nitric oxide donator type telmisartan derivant, preparation method and medical uses thereof The present invention relates to medicinal chemistry, and is especially telmisartan derivatives as NO donor, their preparation process, medicinal compositions containing these compounds or their pharmaceutically acceptable salt or ester, and their medicinal use, especially as medicine for treating metabolic syndrome and relevant diseases.
CN102675105A Phenolic compound in tobacco as well as preparation method and application thereof The invention provides a phenolic compound in tobacco as well as a preparation method and an application thereof, belongs to the field of tobacco chemical research and particularly relates to a preparation method of a new phenolic compound in tobacco and an application of the compound in an anti-cancer drug. The phenolic compound (5-hydroxy-4-oxo-valeric acid) is obtained by being separated from the tobacco. The preparation method comprises the following process steps : crushing a tobacco sample, repeatedly and ultrasonically extracting with 70 weight percent of acetone and combining extracting solution; concentrating the extracting solution under reduced pressure, standing and filtering a sediment; extracting a filtrate with ethyl acetate to obtain extracted solution of the ethyl acetate; and concentrating the extracted solution into an extract, preliminarily separating the extract with a silica-gel column chromatography, then further separating by adopting a semi--preparative high-performance liquid chromatography to obtain the required compound. The compound has better cytotoxic activity on MKN-28 cells and also has a certain activity on K562 cells and Bel-7402 cells.
CA2820114A1 Compound for the treatment of tumours and tumour metastases The invention relates to a Smoothened receptor ligand which antagonises the Hedgehog pathway, to pharmaceutical compositions and therapeutic applications thereof, processes for obtaining this compound and novel intermediates useful in these processes.
CN1883627A Medicinal powder with grassleaved sweetflag for treating tragomaschalia The invention provides a medicinal powder for removing body odor which is prepared from grassleaved sweetflag rhizome, orpiment, sweet basil, mercurous chloride and broom cypress fruit through the steps of disintegrating, sieving and mixing.
WO2014027078A1 Inhibitor compounds of phosphodiesterase type 10a The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof, where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims and where X is C-R6 or N,Y is C-R7 or N, where R6 and R7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. The compounds of the formula I, the N-oxides, tautomers,the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
US7253168 Substituted 1-benzyl-4-substituted piperazine analogues Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
CN102755326A Application of quetiapine to preparation of medicament for treating glioma The invention discloses an application of quetiapine to preparation of a medicament for treating glioma. As proved by an in-vivo experimental result, the quetiapine can be used for inhibiting the growth of glioma by inhibiting proliferation of glioma cells, and promoting differentiation of glioma cells to oligodendrocytes; and as proved by an in-vitro experimental result, the quetiapine can be used for inhibiting proliferation of glioma stem cells and prompting differentiation and maturation of glioma stem cells to oligodendrocytes, has a glioma-resisting function, can play a role in resisting glioma by taking a glioma stem cell as an effect target, can be used for preparing a medicament for treating glioma, and plays a good role in preventing and treating glioma. The application range of the quetiapine is expanded, the market value of the quetiapine is increased, and a novel medicament is provided for the treatment of glioma.
CN103211785A Acipimox film-controlled slow-release pellet capsule The invention relates to an acipimox film-controlled slow-release pellet capsule. A slow-release film of the acipimox film-controlled slow-release pellet utilizes Eurdragit NE 30D as a film-formation material. A pellet core of the acipimox film-controlled slow-release pellet contains low-substituted hydroxypropyl cellulose having high expansibility, and also contains pharmaceutically acceptable common excipients for the slow-release pellet, wherein preferably, the excipients comprise microcrystalline cellulose and lactose, and the pellet core comprises 10 to 40wt% of the low-substituted hydroxypropyl cellulose. The slow-release film comprises the Eurdragit NE 30D, triethyl citrate as a plasticizer and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit NE 30D to triethyl citrate to talcum powder is 30: 2: 4 and coating weight gain is in a range of 20 to 39%. The acipimox film-controlled slow-release pellet comprises the pellet core containing low-substituted hydroxypropyl cellulose having high water expansibility and thus after absorbing water, the acipimox film-controlled slow-release pellet obviously expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the acipimox film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept prior to expiration date.
CN1803134A Preparation method of magnetic nanometer granule containing mitocin-C The invention provides a process for preparing magnetic nano particles containing mitomycin, which consists of the following steps: (1) dissolving aqueous solution of albumin into magnetic liquid formed by Fe3O4 and water, mixing with mitomycin C to obtain aqueous phase, (2) emulsifying the aqueous phase and oily phase with emulsifying agent, (3) heating the emulsion for 5-60 min at 60-100 deg C for solidification, then collecting the particles through conventional methods. The invention can realize the advantages of {>better dispersion in the system, small grain size and large specific surface area.
US20100069384 5-alkyloxy-indolin-2-one derivatives, preparation thereof and application thereof in therapy The present invention relates to derivatives of 5-alkyloxy-indolin-2-one, their method of production and their therapeutic applications. These novel derivatives have affinity and selectivity for the V2 receptors of vasopressin (“V2 receptors”) and can therefore constitute active principles of pharmaceutical compositions.
US20120196791 Combination therapies using antibacterial aminoglycoside compounds Methods for treating a bacterial infection in a mammal in need thereof, and compositions related thereto, are disclosed, the methods comprising administering to the mammal an effective amount of an antibacterial aminoglycoside compound and a second antibacterial agent.
US7097827 Devices, compositions and methods for the pulmonary delivery of aerosolized medicaments According to the subject invention, dispersible dry powder pharmaceutical-based compositions are provided, including methods for their manufacture and dry powder dispersion devices. A dispersible dry powder pharmaceutical-based composition is one having a moisture content of less than about 10% by weight (% w) water, usually below about 5% w and preferably less than about 3% w; a particle size of about 1.0-5.0 μm mass median diameter (MMD), usually 1.0-4.0 μm MMD, and preferably 1.0-3.0 μm MMD; a delivered dose of about >30%, usually >40%, preferably >50%, and most preferred >60%; and an aerosol particle size distribution of about 1.0-5.0 μm mass median aerodynamic diameter (MMAD), usually 1.5-4.5 μm MMAD, and preferably 1.5-4.0 MMAD. Such composition are of pharmaceutical grade purity.
CN1837210A Specific penicillium ketone compounds, process for preparing same and use thereof The invention relates to a group of Notatone A compounds, method for preparation and use thereof, which is prepared from Penicillium notatum B-62 fungus isolated from Qinghai lake mud samples and has novel structure, experiment has proved that the compounds can be used as cell propagation depressant and antineoplastic agent.
US20110152329 Use of Epothilone Derivatives for the Treatment of Hyperparathyroidism The present invention relates to a method of treating a warm-blooded animal, especially a human, having hyperparathyroidism comprising administering to said animal a therapeutically effective amount of an epothilone derivative of formula I or a pharmaceutically acceptable salt thereof.
WO2014100540A1 Pyrazole substituted imidazopyrazines as casein kinase 1 d/e inhibitors The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
US20070254944 Metformin and a dipeptidyl peptidase IV inhibitor such as vildagliptin; improving glucose control A method for improving glucose control by administering metformin in combination with a DPP-IV inhibitor to a patient in need thereof, in an amount sufficient to control the glucose level over an extended period of time.
WO2007139826A3 Method for elevating prolactin in mammals Methods for elevating and stabilizing prolactin levels in a mammal including methods of treating disorders and conditions associated with reduced serum levels of prolactin are provided. Also provided are methods of using certain synthetic tetrapeptide amides which are peripherally selective kappa opioid receptor agonists to elevate or stabilize serum prolactin levels.
WO2012043533A1 Antihuman ccr7 antibodies, hybridoma, nucleic acid, vector, cell, medicinal composition, and antibody-immobilized carrier The purpose of the present invention is to provide a novel antihuman CCR7 antibody which is useful as a therapeutic agent for tissue fibrosis or cancer, a medicinal composition which comprises the antihuman CCR7 antibody, and so on. Provided is an antihuman CCR7 antibody binding specifically to the extracellular domain of human CCR7, said antihuman CCR7 antibody having a heavy chain CDR3 which comprises an amino acid sequence represented by SEQ ID NO: 7, 17, 27, 37, 47, 57, 67 or 77. Also provided is an antihuman CCR7 antibody which has heavy chain CDRs 1-3 and light chain CDRs 1-3, said heavy chain CDRs 1-3 and light chain CDRs 1-3 respectively comprising amino acid sequences represented by SEQ ID NOS:5-10, 15-20, 25-30, 35-40, 45-50, 55-60, 65-70 or 75-80. Preferably, such an antihuman CCR7 antibody has an activity of blocking CCR7-dependent intracellular signal transduction mechanism that is induced by stimulation with CCR7 ligands. The antihuman CCR7 antibodies according to the present invention are usable as the active ingredient of a therapeutic agent for tissue fibrosis or cancer.
CN201572341U Compound amlodipine besylate atorvastatin calcium tablet The utility model discloses a compound amlodipine besylate atorvastatin calcium tablet, which comprises a film coat layer (1) and an amlodipine besylate atorvastatin calcium double-layer tablet (2). The double-layer tablet (2) is directly coated with the film coat layer (1). The amlodipine besylate atorvastatin calcium double-layer tablet (2) consists of an upper layer of amlodipine besylate tablet (3) and a lower layer of atorvastatin calcium tablet (4). The compound amlodipine besylate atorvastatin calcium tablet can ensure simultaneous dissolution of amlodipine besylate and atorvastatin calcium, which is helpful for dosage control; and the tablet has smooth and esthetic appearance and is easy to ingest, so that the compliance of patients is improved.
CN101530389A Ginsenoside Rg 3 and phospholipid complex and preparing method thereof The invention discloses a ginsenoside Rg 3 and phospholipid complex and a preparing method thereof, belonging to the filed of medicines and health care products. The components comprise ginsenoside Rg 3 and phospholipid, and the mol ratio of the ginsenoside Rg 3 to the phospholipid is 1 : 1 to 10. The preparing method adopts organic solvent with small dielectric constant to dissolve the mixture of the ginsenoside Rg 3 and the phospholipid, and then the ginsenoside Rg 3 and phospholipid complex is prepared after the technical processes of solvent evaporation and the like. The ginsenoside Rg 3 and phospholipid complex has fat solubility and high bioavailability, and can be easily absorbed by human bodies and made into preparations such as emulsion and the like.
WO2006019673A3 Jiadifenin analogs and uses thereof The present invention provides compounds having formula (I) and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of neurodegenerative disorders, wherein R1-R6, m and n are as defined herein.
CN101829058A Method for preparing helicid liposome The invention relates to a method for preparing helicid liposome, which comprises the following steps of: weighing and uniformly mixing the helicid and buffer solution of phosphoric acid with a pH value of 6 to 8 in the mass ratio of 1:300-20,000 to obtain the buffer solution of phosphoric acid of the helicid; weighing and uniformly mixing cholesterol, yolk lecithin, soybean lecithin and ethanol in the mass ratio of 1: 0.2-2.5: 0.1-1: 100-800, and distilling the mixture on a rotary evaporator for removing the ethanol to obtain a lipid dry membrane; dissolving the lipid dry membrane in ether, and then adding the buffer solution of phosphoric acid of the helicid, wherein the mass ratio of the ether to the cholesterol is 300-3,000:1; the mass ratio of the buffer solution of phosphoric acid of the helicid to the cholesterol is 100-1,500:1; performing ultrasound processing on the mixture for 5 to 60 minutes, and rotationally evaporating the mixture at the temperature of between 10 and 20 DEG C for removing the ether; and finally, rotationally incubating the mixture in a water bath at the temperature of between 20 and 50 DEG C for 1 to 2 hours to obtain the helicid liposome. The helicid liposome has the advantages of high targeting performance, slow releasing performance, low toxicity and biocompatibility, and contribution to medicament absorption and improvement on bioavailability of medicament.
CN102048677A Valganciclovir Hydrochloride solid preparation and preparation method thereof The invention relates to a Valganciclovir Hydrochloride solid preparation and a preparation method thereof. The Valganciclovir Hydrochloride solid preparation comprises (1) Valganciclovir Hydrochloride, (2) polymer material, and (3) preparation auxiliary material. The Valganciclovir Hydrochloride solid preparation has the advantages of high safety, good absorption property, and high bioavailability. Compared with that the conventional Famciclovir adopts intravenous injection mode for use, the invention provides patients with a better choice and avoids safety hazards caused by injection.
WO2013091052A1 Molecular compound comprising an acridine molecule chemically linked to a carboxylic group, which can be used for the selective destruction of solid tumour cells The present invention relates to oncology, in particular to a molecular compound denominated here as "oncoloose", which is capable of selectively destroying solid tumour cells without affecting rapidly replicating healthy cells. The present invention provides a product comprising a molecular compound denominated oncoloose, which is selectively targeted to the interior of tumours by means of a carboxylic group that neutralizes the negative electrical charge thereof, for transporting the acridine drug to the DNA in the tumour cells, preventing the replication thereof and causing apoptosis or cellular self-destruction of the tumour cells.
CN103284949A A kitasamycin antimicrobial nanoemulsion drug and a preparation method thereof A kitasamycin antimicrobial nanoemulsion drug and a preparation method thereof. The kitasamycin antimicrobial nanoemulsion drug is a composition having a particle size range of between 1nm to 100nm and comprising 0.1%-5% by weight of kitasamycin, 0.1%-8% by weight of an oil phase, 25%-40% by weight of a surfactant, and 4%-25% by weight of a cosurfactant, and the balance water. Combining the composition with the preparation method, the kitasamycin antimicrobial nanoemulsion drug with high bioavailability, low toxic and side effects, good stability, and good palatability is obtained.
US7956040 Combination of catechin and quercetin for pharmaceutical or dietary use The invention relates to a composition for pharmaceutical or dietary use that possesses antioxidant activity and characterized in that it contains as active principle a combination of catechin quercetin, which exert a synergistic action when combined in mutual molar ratios selected within a critical range, from 6:1 to 3:1 mol of catechin:quercetin.
CN102872349A Asthma medicine Cardinal symptoms of a patient suffering from asthma are coughing, breath obstruction, and expectoration sometimes with blood-stained sputum, and severe asthma even causes tracheal rupture and lung duct rupture. The patient suffering from asthma cannot walk for a long time and has difficulty in going up stairs, and severe patients even have a troubled daily life. An asthma medicine comprises three groups of medicines and also has three groups of medication, namely medication of Huafengdan (the first group), which is an ancient prescription passed down from over three hundred years ago, is the main prescription for dozens of chronic diseases and can have different formula and remove wastes and toxins in the lung and the tracheal; medication of medicinal herbs(the second group)which have the efficacies of anti-inflammation, refreshing and enhancement of resistance; and medication of medicinal liquor (the third group) which is made by soaking Chinese eaglewood, bat and gecko in wine, has small toxicity, can combat poison with poison and can remove toxins in the lung and the tracheal. The invention discloses the asthma medicine comprising the three groups of medicines. The asthma medicine has the technical characteristics that the first group of medicines needs to be taken once each month, the second group of medicine needs to be taken for five days each month, the third group of medicine needs to be taken for five days, and the asthma medicine needs to be taken continuously for three months.
WO2013178565A1 Genotype- or phenotype-based drug formulation The invention relates to a combination of two or more pharmaceutically active substances, of which at least one is a metabolic product ("metabolite") of the other ("parent substance"), in particular wherein the dosages thereof are selected in such a way that a genotypically or phenotypically determined variability of the conversion of the parent substance into the metabolite in certain individuals is compensated.
CN102240277A Pharmaceutical composition for treating periodontitis, and preparation method and application thereof The invention relates to a pharmaceutical composition for treating periodontitis and a preparation method thereof, wherein the pharmaceutical composition comprises chlorhexidine or derivatives thereof, poloxamer 407, a release speed adjusting agent, a stabilizer and other additives. The pharmaceutical composition has particular physical characteristics; when the temperature reaches the gel point, the composition can undergo phase transition from liquid to semisolid gel; the composition is liquid at the room temperature; after being used, the composition changes into semisolid gel quickly under the human body temperature condition and then is adhered on the surface of periodontal mucosa to release the medicine, thus a therapeutic effect is obtained; the composition has specific controlled-release property, and can achieve a controlled-release effect of 4 to 5 days of sustained medicine release by adjusting types and dosages of the release speed adjusting agents, thereby reducing the medicine using times, and improving the medication compliance of patients; and the composition is good in stability, and convenient to produce, transport and store.
US20070237834 Zinc Zeolite for the Treatment for Diaper Rash (Diaper Dermatitis) The present invention provides treatment of infants and incontinent adults related to diaper rash, also known as diaper dermatitis, by the application of divalent metal complexes of zeolites, such as zinc zeolite, and compositions thereof.
CN103664884A Tyrosine kinase inhibitor for nitrogen hetero-aromatic ring and derivatives thereof The invention belongs to the technical field of medicines, and particularly relates to a tyrosine kinase inhibitor for nitrogen hetero-aromatic ring and derivatives thereof shown in the general formula (I), and pharmaceutically acceptable salts or stereoisomer thereof, wherein R1, R2, R3, L1, L2, a, b, c, d, e, p, q, A and B are defined in the specification. The invention further relates to a preparation method for the compounds, and pharmaceutical preparations containing the same, and the compounds play an important role in preparing drugs for preventing and/or treating blood cancers (such as B cell chronic lymphocytic leukemia, non-hodgkin lymphomas and the like) related to B cells, and autoimmune diseases (such as thrumatoid arthritis, systemic lupus erythematosus and the like).
US20120277213 Ethynyl compounds The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3′, R4, R4′, R5, R6, R6′, m, and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.
CN1861044A Voriconazole injection and its prepn. method A voriconazole injection contains voriconazole, non-water solvent or its composition and the water for injection, and is prepared through dissolving voriconazole in said non-water solvent, adding the water for injection, regulating pH value, adsorbing impurities and heat source by activated carbon, fine filtering, pouring in containers and sterilizing.
US20100255083 Controlled-release pharmaceutical formulation and process for its preparation The present invention relates to a controlled-release pharmaceutical formulation comprising at least one active ingredient dispersed in a matrix comprising at least one slow-release excipient comprising an association of at least one glycogen and at least one alginate with alkaline-earth metal salts, and a process for its preparation. The invention also relates to a slow-release excipient comprising an association of at least one glycogen and at least one alginate with alkaline-earth metal salts, and the process for its preparation, and its use for the preparation of slow-release pharmaceutical formulations.
US7067527 Thienopyridine derivatives, their production and use The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, —(CH2)q—, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.
CN102020547A PTP1B (Protein Tyrosine Phosphatase 1B) inhibitor as well as chemical synthesis method and application thereof The invention relates to a PTP1B (Protein Tyrosine Phosphatase 1B) inhibitor as well as a chemical synthesis method and application thereof. The chemical structural formula of the PTP1B inhibitor is shown as the description, wherein the group connected with 2,2',3,3',6-position carbon of benzene ring is a bromine atom; 4,4',5,5'-position carbon is connected with methoxy; and the chemical name of the PTP1B inhibitor is (2',3'-dibromo-4',5'-dimethoxy-phenyl)-(2,3,6-tribromo-4,5-dimethoxy-phenyl)-ketone. Through inhibiting the PTP1B activity and increasing the susceptibility of an insulin receptor, the compound has favorable therapeutical effect on insulin resistance type 2 diabete.
WO2013068467A1 Substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with a co-containing group as vanilloid receptor ligands The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with a CO-containing group as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
CN102247351A Preparation method of morin-7-sodium sulfovinate and applications thereof in preparing antithrombotic medicaments and health products The invention belongs to a preparation method of morin-7-sodium sulfovinate and applications thereof in preparing antithrombotic medicaments and health products. The morin-7-sodium sulfovinate can be applied in preparing anti-platelet aggregation and antithrombotic medicaments and health products, or used as the component of the anti-platelet aggregation and antithrombotic medicaments and health products, or used as a precursor of the anti-platelet aggregation and antithrombotic medicaments for reconstruction. The artificially semi-synthesized morin-7-sodium sulfovinate can obviously inhibit platelet aggregation and prevent thrombosis, thus having good anti-platelet aggregation and antithrombotic effects.
CN1562008A Pyrithioxine hydrochloride injection and its preparing method An injection of cervitalin hydrochloride for treating neuropathy and psychosis is prepared from hydroxypropyl-beta-cyclodextrin, Na2EDTA and cervitalin hydrochloride.
CN101195638A Trinuclear phosphamide ester compounds containing tegafur and aza-silicon The invention provides a preparation method of phosphoramidate compound, which comprises materials and a three-necked bottle. The invention uses alkoxy (or phenoxy) phosphorodichloridate as material to be reacted with N3-hydroxyethyl tegafur and aminopropyl nitrogen heterocyclic tricyclic silicon, to synthesize the compound containing tegafur and nitrogen heterocyclic tricyclic silicon. According to the activity splice theory of drug synthesis, the compound has a little toxic and side effects, persistent efficacy, simple synthesis method, low cost, industrialization suitability and the ability for treating colon cancer and gastric cancer, as one anti-tumor agent.
US20130005742 Substituted Diphenylpyrazine Derivatives This invention relates to novel substituted diphenylpyrazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a PGI2 receptor agonist.
CN103142538A PGMS (Propylene Glycol Mannate Sulfate) enteric tablet and preparation method thereof The invention discloses a PGMS (Propylene Glycol Mannate Sulfate) enteric tablet and a preparation method thereof. The PGMS enteric tablet disclosed by the invention consists of a PGMS tablet core and an enteric coating layer coated outside the PGMS tablet core, wherein the PGMS tablet core comprises PGMS, filler and a disintegrant, and the enteric coating layer comprises an enteric material, a plasticizer, an antisticking agent and an opacifier; and during preparation, the PGMS enteric tablet is prepared through coating the enteric coating layer outside the PGMS tablet core. According the PGMS enteric tablet and the preparation method of the PGMS enteric tablet, the enteric effect is ideal, the bioavailability can be improved, and the stimulation to gastric mucosa caused by the drug is reduced; and the preparation method is simple, the quality of obtained products is stable, and thus, the method is applicable to large-scale production application.
US7186711 Can be administered orally or parenterally, in small intervals until an effective dose is achieved The invention relates to the use of flumazenil to produce a medicament for the treatment of cocaine dependency. The flumazenil can be administered sequentially in small quantities at short intervals until a therapeutically effective quantity for the treatment of cocaine dependency has been administered.
EP1827410A2 Bis(thio-hydrazide amides) for increasing hsp70 expression A method of treating a Hsp70-responsive disorder in a subject includes administering to the subject an effective amount of a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt or solvate thereof. Formula (I) Y is a covalent bond or an optionally substituted straight chained hydrocarbyl group, or, Y, taken together with both >C=Z groups to which it is bonded, is an optionally substituted aromatic, group. R1-R4 are independently -H, an optionally substituted aliphatic group, an optionally substituted aryl group , or Rl and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R7-R8 are independently -H, an optionally substituted aliphatic group, or an optionally substituted aryl group. Z is 0 or S.
CN103502226A Cycloalkenyl aryl derivatives for CETP inhibitor The invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the invention show the effect of CETP activity inhibition, which means the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
US20110319451 5-Ht6 Receptor and Modulators Thereof for the Treatment of Insulin-Related Disorders The present invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a candidate compound with a 5-HT6 receptor, b) determining whether 5-HT6 receptor functionality is increased, and c) determining whether a glycemic marker is directly modulated, where an increase in 5-HT6 receptor functionality and direct modulation of a glycemic marker identifies the candidate compound as the glycemic stabilizing compound. In addition, the invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a single dose of a candidate compound with a 5-HT6 receptor, b) determining whether 5-HT6 receptor functionality is increased, and c) determining whether a glycemic marker is directly modulated, where an increase in 5-HT6 receptor functionality and direct modulation of a glycemic marker identifies the candidate compound as the glycemic stabilizing compound. Further, the invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a candidate compound with a 5-HT6 receptor in an isolated cell, b) determining whether 5-HT6 receptor functionality is increased, and c) determining whether a glycemic marker is directly modulated, where an increase in 5-HT6 receptor functionality and direct modulation of a glycemic marker identifies the candidate compound as the glycemic stabilizing compound.
US20120136040 Hybrid interfering rna The invention relates to a hybrid interfering RNA molecule comprising a duplex RNA and a single stranded DNA molecule and its use in the ablation of mRNA and in polymerase chain reactions.
CA2337804C Benzimidazoles, the preparation thereof and their use as pharmaceutical compositions The invention relates to novel benzimidazoles of general formula (1), wherein R a to R c, A, Ar and B have the meanings given in Claim 1, to tautomers, stereoisomers, mixtures and pro-drugs thereof, derivatives thereof containing a group which is negatively charged under physiological conditions in place of a carboxy group, and salts thereof, especially their physiologically compatible salts with inorganic or organic acids or bases with useful properties. The compounds of general formula (I) above wherein R c represents a cyano group are useful intermediate products for the production of the other compounds of general formula (I) and the compounds of general formula (I) wherein R c represents one of the amidino groups cited in Claim I have useful pharmacological properties, especially an antithrombotic effect.
CN1800182A N2-arylformyl-4-ammonia/amidopteridine analog compound capable of regulating nitrous oxide synthase acitivity The invention relates to a method for designing and synthesizing N2-fragrant formyl-4-amido /amido-pteridines derivation with Nitric Oxide Synthase, which has the structure of (I), wherein R1 and R2 at least has one fragrant formyl. The pteridines compound can adjust the activity of NOS and can prepare for the drug.
EP1051655B1 Methods and apparatus for accelerated orthokeratology An accelerated method of orthokeratology includes the steps of softening of the cornea (10) with a softening agent, applying a mold (36) to reshape the cornea (10) to a desired anterior curvature, and rapidly restabilizing or 'fixing' the corneal tissues so that the cornea retains its new configuration. A chemical softening agent, such as glutaric anhydride is applied to the cornea (10) to soften the cornea, after which a specially designed mold (36) of predetermined curvature and configuration is applied to the cornea. Pressure is applied to the mold to re-shape the cornea. The mold (36) is maintained in position while a stabilizing agent, such as a UV light source (96), is positioned above the mold (36). The stabilizing agent, i.e. UV light, is applied to the cornea (10) wherein the stabilizing agent immediately restabilizes the corneal tissue so that the cornea retains its shape upon removal of the mold (36).
EP0647137B1 Glycine receptor antagonists and the use thereof Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating psychosis are disclosed by administering to an animal in need of such treatment a compound having high affinity for the glycine binding site, lacking PCP side effects and which crosses the blood brain barrier of the animal. Also disclosed are novel 1,4-dihydroquinoxaline-2,3-diones, and pharmaceutical compositions thereof. Also disclosed are highly soluble ammonium salts of 1,4-dihydroquinoxaline-2,3-diones.
EP1786264A2 Cationic antiseptic compositions and methods of use Antimicrobial compositions, especially those useful when applied topically, particularly to mucosal tissues (i.e., mucous membranes), including a cationic antiseptic such as biguanides and bisbiguanides such as chlorhexidine and its various salts including but not limited to the digluconate, diacetate, dimethosulfate, and dilactate salts; polymeric quaternary ammonium compounds such as polyhexamethylenebiguanide; silver and various silver complexes; small molecule quaternary ammonium compounds such as benzalkoium chloride and alkyl substituted derivatives; di-long chain alkyl (C8-C18) quaternary ammonium compounds; cetylpyridinium halides and their derivatives; benzethonium chloride and its alkyl substituted derivatives; and octenidine. The compositions can also include an enhancer component, a surfactant, a hydrophobic component, and/or a hydrophilic component. Such compositions provide effective topical antimicrobial activity and are accordingly useful in the treatment and/or prevention of conditions that are caused, or aggravated by, microorganisms (including viruses).
WO2008155069A2 Substituted oxazolidinones and use thereof The invention relates to novel, substituted oxazolidinones, methods for the production thereof, use thereof for the treatment and/or prophylaxis of diseases, and the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.
CN101829117A Application of evodiamine in preparation of medicaments for treating alzheimer disease The invention belongs to the field of medicaments, and provides the application of evodiamine in preparation of medicaments for treating alzheimer disease. The evodiamine can improve main symptoms of alzheimer disease, namely loss of learning and memory capability. The delay of the progression of alzheimer disease is mainly realized by: 1, inhibiting excessive activation of microglia in brain tissues, and lowering over-expression of cytokines IL-1, IL-6 and TNF-alpha; and 2, lowering expression of cycloxygenase-2, and inhibiting an inflammatory reaction of the central nervous system. Researches of curative effect and molecular mechanism on the evodiamine treating alzheimer disease prove that the evodiamine has quite good treating effect and has huge potential of becoming a clinical treatment medicament.
CN102847024A Haemostatic medicine The invention discloses a haemostatic medicine comprising the raw materials of, by mass: 1-2 parts of common burreed tuber, 4-8 parts of cochinchinese asparagus root tuber, 1-3 parts of common wedgelet fern leaf, 2-4 parts of spirifer shell fossil, 1-3 parts of willowleaf swallowwort rhizome and root, 1-2 parts of henon bamboo leaf, 2-6 parts of red peony root, 0.2-0.6 parts of oyster, 2-5 parts of immature tangerine fruit, 3-8 parts of rosewood heart wood, 1-3 parts of immature bitter orange, 2-4 parts of gradfly, 0.4-0.6 parts of Mongolian milkvetch root, 1-3 parts of pilose asiabell root, 1-2 parts of gold theragran, 2-4 parts of hairy antler pilose antler, 2-9 parts of Japanese pogodatree flower, 1-5 parts of songaria cynomorium herb, 3-7 parts of hematite, 4-6 parts of thymifoious euphorbia herb, 0.1-0.5 parts of Chinese soapberry fruit, 1-4 parts of fringed pind herb, and 1-2 parts of Indian adenosma herb. The haemostatic medicine provided by the invention has the functions of liver calming, yang suppressing, adverse-qi calming, qi promoting, blood circulation activating, blood cooling, and bleeding stopping. The medicine also has the functions of heat clearing, restless arresting, body fluid regenerating, diuresis promoting, yin nourishing, heat clearing, lung moistening, and kidney nourishing.
EP2318369A1 Squaric acid derivatives as inhibitors of the nicotinamide The present application discloses novel squaric acid derivatives of the formula A: from -C(=O)-, -S(=O)2-, -C(=S)- and -P(=O)(R5)-; B: -, -O-, -NR6- and -C(=O)-NR6-; D : -, -O-, -CR7R8- and -NR9; m=0-12; n = 0-12; m+n = 1-20; p=0-2; R1 : heteroaryl, aryl; R2 : H, C1-12-alkyl, C3-12-cycloalkyl, -[CH2CH2O]1-10-(C1-6-alkyl),C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3 : C1-12-alkyl, C3-12-cycloalkyl, -[CH2CH2O]1-10-(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3 : N-containing heterocyclic/heteroaromatic ring; R4 and R4* : H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and viral infections, adult respiratory distress syndrome, ataxia telengiectasia).
WO2011115527A8 New biologically active compound n-[3-(4-nitrophenylamino)-indol-2-ylmethylene]aminoguanidine hydrochloride with anti-inflammatory activity The invention relates to the field of the pharmaceutical chemical industry and medicine. N-[3-(4-nitrophenylamino)-indol-2-ylmethylene]- aminoguanidine hydrochloride of formula (2), which possesses anti-inflammatory and chondroprotective activity, is proposed. The compound does not exhibit side-effects when used.
US6921774 Administering compounds such as N-(3-(5-Cyano-1-(4-fluoro-phenyl)-1,3-dihydroisobenzofuran-1-yl)-1 -propyl)glycine ethyl ester, for prophylaxis of psychological disorders The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.
CN102190659A Phenylpyrazine compounds, and preparation method and medicinal application thereof The invention discloses phenylpyrazine compounds, and a preparation method and medicinal application thereof. The phenylpyrazine compounds are inhibitors capable of selectively targeting dipeptidyl peptidase-4, and have medicinal application to preventing or treating diabetes (particularly type II diabetes), hyperglycemia, X syndrome (microvascular angina), hyperinsulinemia, obesity, atherosclerosis and various immune-mediated diseases.
US20100331278 Uses of cationic hydroxyethylcellulose in oral ingestion forms, and prevention and treatment of metabolic disorders Described are an oral ingestion form comprising cationic hydroxyethylcellulose, and methods of using the same in prevention and treatment of metabolic disorders.
CN101899076A Azithromycin derivative, preparation method and intermediate thereof The invention discloses an azithromycin derivative shown in the formula (I) and a pharmaceutically acceptable salt thereof, wherein R1 represents hydrogen, acetyl or benzoyl, R2 represents hydrogen, aliphatic hydrocarbon, substituted aromatic alkyl, substituted aromatic heterocyclic alkyl, halogen, nitryl, alkoxy or-AR7, R3 represents OR5, R4 represents hydroxyl; or, R3 and R4 can form a ring with a structure that X represents oxygen and nitrogen; R5 represents nitrogen or CONHR6, R6 represents aliphatic hydrocarbon, substituted aromatic alkyl or substituted aromatic heterocyclic alkyl, and R7 represents aliphatic hydrocarbon, substituted aromatic alkyl or substituted aromatic heterocyclic alkyl; n is from 1 to 6, A is one of -O-,-CO-,-CONR8-,-NHCO- and -S-. The invention further relates to a prepared intermediate and a method thereof, an acceptable salt thereof forming with inorganic or organic acid, a drug composite and application thereof in the treatment of bacterial infection.
WO2013135189A1 Solid dispersion improving absorption performance and preparation of same Provided are a solid dispersion improving absorption performance and a method for preparing same. Specifically, a solid dispersion is provided, comprising (A): a compound of Formula A as an active ingredient or a derivant thereof, or a pharmaceutically acceptable salt, a hydrate or a solvate thereof; and (B): a hydrophilic high polymer carrier. A weight ratio of (A) to (B) ranges from 1:1 to 1:40. The solid dispersion according to the present invention can significantly improve a vitro dissolution of the active ingredient and remarkably improve absorption of a mammal for the active ingredient, thereby effectively reducing the dosage thereof in use.
WO2009130604A3 Solid state forms of deferasirox salts and process for the preparation thereof Provided herein are novel solid state forms of deferasirox salts, process for the preparation, pharmaceutical compositions, and method of treating thereof. The solid state forms of deferasirox salts are useful for preparing deferasirox (I) in high purity.
CN103120643A Curcumin dicaprate suspension injection and preparation method and application thereof The invention discloses curcumin dicaprate and a derivative nano suspension agent, a preparation method of freeze-dried powder thereof and an application in the treatment of depression and tumor. A surfactant serves as a main pharmaceutical adjunct, particularly poloxamer, and curcumin dicaprate nano granulation is successfully realized by employing the wet grinding combined freeze drying technology. The curcumin dicaprate is prepared into a pharmaceutically acceptable oil diluent, and the reconstructed curcumin dicaprate and derivative nano suspension agent can be prepared into a nano suspension agent for injection with the particle size of about 500nm. The nano suspension agent consists of the following components: curcumin dicaprate and/or derivatives thereof and the surfactant. The nano suspension agent preparation can be applied to treating depression and tumors. The nano suspension agent preparation is simple in composition, high in stability, high in needle penetration, economic and reliable in preparation method and easy to industrialize.
CN101491533B Use of baicalin in preparing medicine The invention relates to application of scutelloside in pharmacy. The scutelloside promotes a T cell to be transformed toward Treg with immunological suppression effect by up-regulating the expression of Foxp3; at the same time, the scutelloside inhibits Th17 with pro-inflammatory effect and inhibits vasculitis mediated by the Th17. A main mechanism of inhibting the Th17 of the scutelloside is toinhibit the amplification of the Th17 mediated by IL-6. At the same time, a further experiment proves that the scutelloside taken as a novel immunomodulator plays good therapeutic effect on treating lupus erythenlatosus nephritis and rheumatoid arthritis.
US20100098794 Topical anti-wrinkle and anti-aging moisturizing cream The present invention relates to a topical anti-wrinkle and anti-aging moisturizing cream designed (formulated) to repair and restore human adult skin to its original youthful state. This has successfully been achieved by using a water based molecular mixture of high molecular weight (0.5 to 2.0 million Daltons) hyaluronic acid (HA) and of low molecular weight hyaluronic acid oligosaccharides (small HA fragments less than 12000 Daltons molecular weight) to create this unique anti-aging moisturizer. An equal mixture of high molecular HA and HA-oligosaccharides at concentrations of 0.1-0.2% was found to be essential for providing our moisturizer its unique ability to repair and rejuvenate adult human skin.
US20130040932 Substituted aryl sulfone derivatives as calcium channel blockers A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
CN101074234B Antitumor antibiotics and its production A pyranyl nequinone anti-neoplastic antibiotic is prepared by fermenting, culturing Nocardiopsis sp. YIM 80133, separating out from fermented liquid, purifying extract to obtain final product with molecular formula C21H20010 and molecular weight 432.38. It has strong inhibiting function of human progranuleukemic tumor cell.
CN103239533A Flavoured qi infusing decoction for treating simple intestinal obstruction and preparation method thereof The invention provides a flavoured qi infusing decoction for treating simple intestinal obstruction and a preparation method thereof, aiming at solving the problem that the ancient prescription dachengqi decoction can damage spleen and stomach and belonging to the field of medicines for treating intestinal obstruction. According to the flavoured qi infusing decoction, Chinese angelica is added on the basis of the dachengqi decoction (9g of mirabilite, 12g of rheum officinale, 12g of immature bitter orange and 15g of mangnolia officinalis), so that the flavoured qi infusing decoction has the effects of moistening dryness, activating blood, removing blood stasis and relaxing bowel; the Chinese angelica can be used for tonifying middle-jiao and qi and partially eliminating the adverse effect of deficiency-cold in spleen and stomach caused by rheum officinale and mirabilite; then codonopsis pilosula, walnut kernel, bee glue and honey are added to further enhance dryness moistening and bowel relaxing effects; the codonopsis pilosula can be used for tonifying middle-jiao and qi and eliminating the adverse effect of deficiency-cold in spleen and stomach caused by rheum officinale and mirabilite; the bee glue also can be used for sterilizing and improving the organism immune capacity; and the honey can be used for regulating taste of decoction. Therefore, the flavoured qi infusing decoction for treating the simple intestinal obstruction has the advantages of quick effect and small damage on organisms.
CN102532024A Sinomenine derivative The invention discloses a sinomenine derivative and salt acceptable by pharmacy, and a sinomenine-containing derivative and a drug synthesis of salt acceptable by pharmacy and application thereof. The sinomenine derivative and the salt acceptable by pharmacy are prepared through a chemical synthesis method with sinomenine as a parent compound, have remarkable effects on analgesia, anti-inflammation and relieving cough, are obviously superior to sinomenine, and can be used for curing related diseases.
EP1699490A2 Medical lipolysis of fat accumulations The invention relates to aqueous compositions, comprising at least one phospholipid and/or at least one bile acid and a component such as riboflavin or water, supporting the decomposition of fat, which are suitable for the production of medicaments for the removal of subcutaneous fat accumulations and lead to a reduction in the diet-resistant fatty layer.
US20120003309 Solid Dosage Forms Of Bendamustine In the present invention there is provided a pharmaceutical composition in a solid dosage form suitable for oral administration, the composition comprising bendamustine or a pharmaceutically acceptable ester, salt or solvate thereof as an active ingredient, and at least one pharmaceutically acceptable excipient, which is a pharmaceutically acceptable saccharide selected from the group consisting of one or more of a monosaccharide, a disaccharide, an oligosaccharide, a cyclic oligosaccharide, a polysaccharide and a saccharide alcohol, wherein the ratio by weight of the active ingredient to the saccharide excipient(s) is in the range of 1:1-5.
WO2014073904A1 Gpr40 receptor agonist, methods of preparing the same, and pharmaceutical compositions containing the same as an active ingredient The present invention relates to a novel compound having GPR40 receptor agonist activity that promotes insulin secretion and inhibits blood sugar rise after glucose loading, and is thereby useful for the treatment of diabetes and complications thereof, the preparation method thereof and pharmaceutical composition containing them as an active ingredient.
EP1881984B1 Inhibitors of nucleoside phosphorylases and nucleosidases The present invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5'-methylthioadenosine phosphorylases (MTAP), 5'-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.
US20090099215 Metabolic enhancing properties of norphenephrine and its salts Norphenephrine and its salts are disclosed which have powerful metabolic enhancing effects in humans via oral administration. The metabolic enhancing properties include positive blood sugar regulation, increased thermogenesis and fat loss, increased anticatabolism/anabolism, decreased appetite, improved mental focus and psychological outlook and increased energy production and anti-fatigue actions.
CN102093315A C7 and C10 modified 1-dehydroxyl taxol analogue and preparation method thereof The invention relates to a C7 and C10 modified 1-dehydroxyl taxol analogue and a preparation method thereof. The structural formula of the compound is shown in the specification, wherein R1 is a C1-C8 linear chain or branched alkyl group, a C3-C6 cycloalkyl group, a phenyl group, or a 5--membered or 6-membered aromatic ring containing nitrogen, sulphur or oxygen; and R2 is a C1-C8 linear chain or branched alkyl group or a C3-C6 cycloalkyl group. The structural formula of the analogue is shown in the above formula. In the preparation method, the target product C7 and C10 modified 1-dehydroxyl taxol analogue is synthesized and obtained based on 1-dehydroxyl baccatin VI as a raw material. The obtained product has bioactivity in the aspect of anticancer and has an application prospect in the aspect of drug resistance of taxol. The preparation method has the characteristics of good selectivity, simple post-treatment and high yield.
US20120079613 Homeobox Transcription Factor BSX and Uses Thereof for Treating Diseases, in Particular Obesity The present invention relates to the human homeobox transcription factor Bsx protein, nucleic acids encoding for said protein, vectors and cells comprising the nucleic acids, antibodies directed against Bsx, and methods for identifying compounds binding to Bsx, as well as to the use of proteins, nucleic acids, vectors, cells, and interacting compounds for treating obesity and related diseases.
US20080293761 Pyrrolopyridine-2-Carboxylic Acid Amide Derivative Useful as Inhibitor of Glycogen Phosphorylase The present invention is directed to a novel form of a pyrrolopyridine-2-carboxylic acid amide of formula (I), which is an inhibitor of glycogen phosphorylase, compositions containing it and their use in therapy. The invention is also directed to processes for production of the novel form, novel intermediates used in said processes and processes for the production of said intermediates.
CN101112620B Cisplatin-hydroxyapatite -chitose sustained-release microsphere and uses thereof The present invention relates to a cisplatin - hydroxyapatite-chitosan sustained release microsphere, the shape is a sphere, the sphere diameter is 5 Mum-20 Mum; the components are cisplatin (DDP), hydroxyapatite (HAP) and chitosan (CS), the weight percentage of the cisplatin is 10 to 20 percent, the weight percentage of hydroxyapatite is 10 to 30 percent and the weight percentage of chitosan is 50 to 80 percent; the structure is that the mixture of cisplatin, hydroxyapatite and chitosan is coated with an outer shell which is formed by chitosan. The experiments show that the sustained releasemicrosphere can be used in chemotherapy, which can reduce the toxicity and the side effects to the normal tissues, play the anti-tumor effect sustainedly in a longer term and particularly improve theefficacy for the ovarian cancer.
EP1737455A1 Controlled release pharmaceutical composition of tolperisone for oral administration The invention relates to a tolperisone-containing pharmaceutical preparation with controllable active-substance release for oral administration, characterised in that the active substance tolperisone and/or a pharmaceutical salt thereof is embedded in a pharmaceutically compatible material. By selecting the pharmaceutically compatible materials in the preparation and accordingly in the coating of a tablet or granule, a specific release of active substance can be adjusted which is matched to the special genotype in the metabolisation of tolperisone. At the same time, as a result of the very uniform and persistent release of tolperisone, the in-vivo inversion of enantiomerically pure tolperisone that is known from the art can be adjusted in favour of the R(-) tolperisone which is prominent in muscle-relaxing therapy.
EP1980261A1 Use of helium with oxygen to provide neuroprotection Helium is used to provide neuroprotection, in particular in patients having suffered an impact trauma to the head and/or spinal column.
EP1833780A1 Methods of making pravastatin sodium The invention encompasses a new crystalline form of pravastatin sodium characterized by X-ray powder diffraction peaks at 3.3, 3.9, 5.4, 6.4, 16.8, and 17.5 degrees two-theta, ± 0.1 degrees two-theta and to methods of forming the crystalline form of the present invention and methods of making pravastatin Form B and Form D.
CN101574455B Mongolian dandelion herb and parslane herb decoction used for clearing away acute mastitis The invention relates to the field of medicament formulas, in particular to Mongolian dandelion herb and parslane herb decoction used for clearing away acute mastitis, which is prepared by the following steps: firstly separately packaging mirabilite, cleaning Mongolian dandelion herb, parslane herb, cholla stem, plaster, honeysuckle, weeping forsythiae capsule, corktree leaf, officinal magnolia bark, pinelliatuber, and Chinese gall, soaking by water, decocting to remove slag so as to obtain filter liquor, then adding the mirabilite, and decocting by low fire for one or two boiling to prepare the decoction. The Mongolian dandelion herb and parslane herb decoction is characterized in that: the raw materials by weight percentage are 18 to 21 percent of the Mongolian dandelion herb, 15 to 18 percent of the parslane herb, 11 to 13 percent of the cholla stem, 5 to 7 percent of the plaster, 8 to 11 percent of the honeysuckle, 5 to 8 percent of the weeping forsythiae capsule, 7 to 9 percent ofthe Chinese gall, 5 to 7 percent of the corktree leaf, 4 to 7 percent of the officinal magnolia bark, and 4 to 7 percent of the pinelliatuber. The Mongolian dandelion herb and parslane herb decoctionfor treating the acute mastitis has low cost, high curative effect of clearing away the acute mastitis, and no toxic and side effects, has effects of diminishing inflammation, resisting infection andstrengthening immunity of organisms, and is suitable for early and metaphase acute mastitis.
WO2010057028A9 Treatment of proteinopathies using a farnesyl transferase inhibitor Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject in need thereof a therapeutically effective amount of a farnesyl transferase inhibitor, wherein the amount is effective to inhibit the farnesylation of a non-Ras FTase substrate involved in the autophagy pathway without substantially affecting the farnesylation of Ras or other oncology related substrates. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant.
US20100087509 Methods, Agents, and Compound Screening Assays for Inducing Differentiation of Undifferentiated Mammalian Cells into Osteoblasts The present invention relates to methods, agents and compound screening assays for inducing differentiation of undifferentiated mammalian cells into osteoblasts. The invention thus provides a method, comprising contacting a compound with a polypeptide comprising an amino acid sequence selected from the group consisting of SEQ ID No: 194-309; and measuring a compound-polypeptide property related to the differentiation of said cells. The invention further relates to a bone formation enhancing pharmaceutical composition, and the use thereof in treating and/or preventing a disease involving a systemic or local decrease in mean bone density in a subject. Furthermore, the invention relates to a method for the in vitro production of bone tissue.
CN101015512B Composition and its application in oral cavity nursing product The invention provides a composition for the prevention and treatment of oral diseases such as periodontitis, stomatitis, halitosis and gingivitis, which comprises (by weight percent) coptis root extract 0.2-4%, and weeping forsythia extract 0.2-8%, borax 85-95% and balancing deionized water. The composition is applicable for preparing oral nursing products such as toothpaste and mouthwash.
CN103463017A Application of Lycojaponicumin B in preparation of medicines for treating pancreatic cancer The invention discloses an application of Lycojaponicumin B in preparation of medicines for treating pancreatic cancer, belonging to the technical field of new applications of medicines. The evaluation on the anti-tumor activity of the Lycojaponicumin B by an MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method in vitro shows that the Lycojaponicumin B also has an obvious inhibiting effect on the growth of human pancreatic cancer cell lines PANC-1 and BXPC-3. Therefore, the Lycojaponicumin B can be used for the preparation of the medicines for resisting the pancreatic cancer and has good development and application prospects. The application of the Lycojaponicumin B in the preparation of the medicines for treating the pancreatic cancer is disclosed by the invention for the first time. As the skeleton type of the Lycojaponicumin B belongs to a brand-new skeleton type, the Lycojaponicumin B has unexpected strong inhibitory activity on pancreatic cancer cells.
US7163699 Progestin co-micronized with a surfactant pharmaceutical composition comprising same methods for making same and uses thereof The invention concerns a progestin co-micronized with a surfactant and a pharmaceutical composition comprising said gestagenic. The invention also concerns methods for preparing same.
CN101708156B Camptothecin medicament injection solution and injection and preparation method thereof The invention relates to the technical field of medicaments, in particular to a camptothecin medicament injection solution and an injection and a preparation method thereof. The invention provides a camptothecin medicament injection which is good in stability, high in curative effect and low in toxicity and consists of the camptothecin medicament injection solution and a disperse medium, wherein the camptothecin medicament injection solution consists of a medicament active component, a stabilizing agent, a pH value regulator and an injection solvent. The medicament active component of the camptothecin medicament injection solution is a camptothecin medicament mainly existing in the form of a lactonic ring, which can improve the curative activity of the medicament and reduce toxic side effects; and the disperse medium is an injection emulsion, which can improve the dispersion degree of the camptothecin medicament and solve the problem that the camptothecin medicament is difficult to beprepared into the injection due to poor water solubility. The camptothecin medicament injection solution and the injection emulsion are packed and then stored respectively, and are mixed uniformly before use for intravenous administration, so the stability of the medicaments stored for a long time can be improved. The invention provides an intravenous injection which has low toxicity and is save and convenient to store for camptothecin medicaments.
CN103705714A Application of cough treatment fritillary and loquat dripping pill in preparation of anti-influenza A virus drugs The invention discloses application of a cough treatment fritillary and loquat dripping pill in preparation of anti-influenza A virus drugs. The cough treatment fritillary and loquat dripping pill is mainly composed of loquat leaves, fritillary bulb, platycodon grandiflorum, Rhizoma Typhonii Flagelliformis and menthol. Experiments prove that the cough treatment fritillary and loquat dripping pill has an inhibiting effect on the influenza A virus, so that an effective drug for clinical treatment of the influenza A virus infection can be provided.
WO2007093608A8 Drug combinations for the treatment of respiratory tract diseases The present invention relates to novel drug combinations which, besides one or more, preferably one, compound of the general formula 1, in which A, B, R1, X, n and m can have the meanings given in the claims and in the description, comprise at least one further active ingredient 2, to methods for the production thereof, and to the use thereof as drugs.
US8333961 Natural liniment for treatment of skin cancers A liniment composition for reversing or retarding the growth of cancerous skin tumors comprising primarily, pancreatin, pepsin, betaine HCL, emulsified vitamin A, and zinc, pancrelipase, fenugreek, papain, amylase and ox bile extract, with optional trace amounts of other ingredients.
CN102697975A Coptis shangqing tablet improved preparation for treating several diseases The invention relates to a coptis shangqing tablet improved preparation for treating several diseases; the improved preparation makes use of the toxin expelling effect, that is, the deficiency fire removing effect of coptis shangqing tablets, and the blood-activating stasis-transforming refreshing and resuscitation-inducing effects of mint in the formula, has a properly-adjusted mint amount, is added with other drugs aiming at several diseases respectively, and can effectively treat cancers, cerebral hemorrhage hemiplegia, mental disorders, and hemorrhoid; the preparation is prepared through mature technology, has a unique formula, realizes the medical principle of syndrome differentiation treatment, has definite therapeutic effect, and low cost, can cure cancers, cerebral hemorrhage hemiplegia, and mental disorders within several months, and can cure hemorrhoid within about four days.
CN103251935A Medicinal composite containing cornu cervi pantotrichum and application thereof The invention discloses a medicinal composite containing cornu cervi pantotrichum. The medicinal composite comprises the following components in percentage by weight: 1%-20% of cornu cervi pantotrichum freeze-dried powder, 1%-10% of glucosamine, 1%-20% of collagen, 1%-10% of vitamins B6, 1%-20% of dolomites and 95%-20% of germinated soybean meal, wherein the sum of drugs is 100%; the cornu cervi pantotrichum freeze-dried powder is prepared through the following steps of: freeze-drying fresh cornu cervi pantotrichum, smashing, extracting at 0-4 DEG C by using normal saline, centrifugalizing an extracting solution, and freeze-drying a supernatant into powder. The medicinal composite disclosed by the invention is prepared into a postmenopausal osteoporosis animal model by adopting a ovariotomy method and continuously applied for 12 weeks, is displayed to be used for preventing and treating cancellous bone losing caused due to estrogen reduction through a result and prompted to correct the bone turnover rate enhancement caused due to low estrogen level and improve the coupling unbalance condition of bone absorption and bone formation through a bone metabolism biochemical index and a bone density result, promotes the bone formation and has certain preventing and treating effects on high-turnover type osteoporosis which takes the cancellous bone losing as a main part.
WO2007077770A1 Alkylresorcinol glycoside, process for production of the same, and use of the same The object is to provide a 4-alkylresorcinol derivative in which defects inherent to a 4-alkylresorcinol are overcome and which is excellent in solubility in water and stability, has substantially no taste and no odor, is not irritative, is free from the concern about toxicity, and can exert its physiological activity in a living body satisfactorily. Thus, disclosed is a 4-alkylresorcinol glycoside which has a glycosyl group attached to one or both of the hydroxyl groups in a 4-alkylresorcinol.
US20120195957 Novel nanoparticle formulations for skin delivery Methods and formulations for treating a condition of the skin by delivering therapeutic formulations to the skin that translocates active substances across the stratum corneum barrier to a targeted skin tissue. The methods and formulations comprise active substances encapsulated within surface modified nanostructured lipid carrier nanoparticles.
WO2014088519A1 Compounds including map kinase interacting kinases 1 and 2 (mnk1 and mnk2) modulators and abl and abl (t315i) inhibitors, and uses thereof The present invention relates to certain piperazine-based compounds that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b and/or as ABL or ABL (T315I) inhibitors. The invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of cancer, inflammatory and Alzheimer disease conditions, as well as methods of treatment of these disorders.
US7524854 Trimethoprim derivative; 5-[6,7-Dimethoxy-2-(7-methoxy-1H-indol-3-ylmethyl)-benzofuran-4-ylmethyl]-pyrimidine-2,4-diamine; potent activity against dihydrofolate reductase, mutated enzyme; superior bioavailability, antibacterial activity; gram positive and negative pathogens The invention relates to new benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.
CN101412719B Carbapenem derivatives The invention belongs to the technical field of medicine, in particular to a carbapenems derivative shown in a general formula (1), pharmaceutically acceptable salts, easily hydrolysable esters or isomers thereof, wherein R<1>, R<2>, R<3>, R<4>, R<5> and R<6> are defined in the specification. The invention also relates to a method for preparing the compounds, medical compositions containing the compounds, and application of the compounds to the preparation of medicines for treating and/ preventing infectious diseases.
EP1499325B1 Composition comprising trehalose and zinc and use thereof to inhibit skin irritation Compositions for reducing an adverse skin reaction caused by a skin-irritating agent or skin sensitizing agent by treatment with a disaccharide and a metal ion, as well as methods for reducing an adverse skin reaction caused by a skin-irritating or skin-sensitizing agent, and methods for treating an inflammatory response to at least one inflammatory agent, by application of a disaccharide and/or metal ion composition.
US20120164067 Methods of preventing or treating pain using anti-ngf antibodies that selectively inhibit the association of ngf with trka, without affecting the association of ngf with p75 NGF antagonists including antibodies and antibody fragments thereof having binding specificity to human Nerve Growth Factor (“NGF”), and methods of treating pain. Methods of treating pain or eliciting an analgesic effect in an individual comprising administering an effective amount of an NGF antagonist inhibits the association of NGF with TrkA without inhibiting the association of NGF with p75. The methods may further comprise administering an effective amount of a second anti-human NGF antibody or fragment thereof which inhibits the association of NGF with p75, that may further also inhibit the association of NGF with TrkA.
WO2014009425A1 Inhibition of enzymes Compounds of formula (I) are inhibitors of neutrophil elastase wherein R1, R2, R3, R5, R6, A1, A2, A3, A4 assume meanings as defined in formula (I).
WO2013034047A1 Heterocyclic-substitued benzofuran derivatives and methods of use thereof for the treatment of viral diseases The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
WO2009035033A1 Ophthalmic composition It is intended to provide an ophthalmic composition which stabilizes the lacrimal fluid layer during wearing contact lenses, prevents eye dryness, imparts a favorable feeling in using, is highly convenient with no risk of misusage and shows a high efficiency in the course from the manufacturing to selling. More specifically, it is intended to provide eyedrops for wearing contact lenses which comprises: (A) one or more members selected from the group consisting of a cellulose-base polymer compound, a vinyl-base polymer compound, polyethylene glycol and dextran; (B) one or more members selected from the group consisting of chondroitin sulfate, alginic acid and salts thereof; and (C) a nonionic surfactant.
CN1565433A Hypocrellin water-soluble nanogranule and its uses The invention relates to a Hypocrellin water-soluble nanogranule and its uses characterized in that, native protein, polysaccharide macromolecule and biodegradable high molecular polymer can be used as packing material, the liposoluble bamboo bacterioerythrin medicament is packed for preparing ultra-microminiature water-soluble intravenous injection with grain diameter of 20-200nm. These preparations can be used as the intravenous injection for optical dynamic medicament of Hypocrellin.
EP2289515A2 Combinations comprising a diaryl urea and an interferon The present invention provides methods for treating cancer in humans and other mammals comprising administering a chemotherapeutic agent, such as an interferon, and an aryl urea compound of Formula (I) : B-NH-C(O)-NH-L-M-L1-(Q)1-3 (I). In Formula (I), B and L and are each, independently, optionally substituted phenyl, naphthyl, a 5 or 6 membered monocyclic heteroaryl group, or an 8 to 10 membered bicyclic heteroaryl group; M is a bridging group. each Q is independently C(O)R4, C(O)OR4 and C(O)NR4R5; and L' is optionally substituted phenyl, naphthyl, monocyclic heteroaryl or bicyclic heteroaryl, or a saturated or partially saturated, monocyclic or bicyclic carbocyclic moiety or heterocyclic moiety.
CN101416935A Preparation method of composite sulfamethoxydiazine suspension The invention relates to a preparation method of a compound sulfametoxydiazine suspension which consists of sulfametoxydiazine, trimethoprim, sodium hydroxide, carboxymethylcellulose sodium, propylene glycol, tween-80 and water used for injection. The preparation method comprises the steps that: (1) the carboxymethylcellulose sodium swells by using 20ml of water used for injection; (2) then the propylene glycol is added; (3) the sodium hydroxide is dissolved with 5ml of water for standby; (4) the products of Step (1) and Step (2) are placed upside down in a beaker, stirred for 5 minutes, added with the trimethoprim, the sulfametoxydiazine and the tween-80 in sequence and stirred while being adding; the sodium hydroxide is used for adjusting and controlling the pH value to be 5.3 to 5.6; finally, stirring is carried out for 30 minutes and volume is fixed to be 100ml by using the water used for injection; and (5) the solution is put into a colloid mill so as to be milled for 10 minutes and sieved by a 200-mesh sieve, thus obtaining the compound sulfametoxydiazine suspension. Veterinary drugs prepared by the method have the advantages of less application times, long-lasting effect, good curative effect, and the like.
US20050004120 Arylmethyl-carbonylamino-thiazole derivatives and their use as antitumor agents A method of modulating apoptosis or treating diseases associated with protein kinases by administering to a mammal in need thereof of an effective amount of 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R1, R2 and R3 are as defined herein, or pharmaceutically acceptable salts thereof.
US20080194703 Method of Preparing Lycopene-Enriched Formulations That are Free of Organic Solvents, Formulations Thus Obtained, Compositions Comprising Said Formulations and Use of Same The present invention refers to a process to obtain a lycopene-enriched formulation free of organic solvents that comprises: (a) mixing a lycopene source with an extractant lipid, and (b) separating the lipidic phase obtained in step (a) to obtain the lycopene-enriched formulation free of organic solvents; in which the mixture in step (a) is carried out in the absence of organic solvents. The invention also refers to the formulations obtained in this way and to compositions that comprise them. These formulations and compositions have antioxidant properties and are useful to manufacture nutraceutical, cosmetic, pharmaceutical or food products.
US20130017174 Compositions and methods for increasing health and reducing pathogenic bacteria in animals Probiotic compositions comprising a bacterium that is capable of producing nitric oxide and a substrate of nitric oxide synthase are provided. Also provided are methods of improving the gastrointestinal health of a subject by orally administering a bacterium capable of producing nitric oxide and orally administering a substrate of nitric oxide synthase. Methods of reducing the inflammatory immune response after treatment with a probiotic and methods of reducing horizontal transmission of pathogenic bacteria within groups of animals are also provided.
CN103656645A Novel molecular target for treating opiate addiction and application thereof in drug development The invention discloses a novel target for developing a drug for treating opiate addiction, namely heat shock protein 70 (Hsp70). The invention discloses a classical evaluation model-single needle morphine-induced rat behavior sensitization for opiate addiction. Hsp70 in addiction-mediated critical nucleus (nucleus accumbens core, NAccore) plays a decisive role at the behavioral sensitization formation phase no matter in transcriptional level or functional level. Therefore, a chemical reagent for restraining the transcriptional level or the functional activity of the Hsp70 can provide a novel treatment method for related diseases of opiate addiction.
US20120251629 Methods of treatment and screening assays for hif-1alpha regulation The present invention relates to a method of treating a patient for a condition where blood flow to a tissue or organ is interrupted. This method involves administering to a patient with a hypoxic condition where blood flow to a tissue or organ is interrupted, or at risk thereof, a compound that reduces the rate of HIF-1α inactivation in cells affected by the condition, thereby treating the patient for the condition. Also disclosed is a method of treating a tumor in a patient. In addition, the present invention relates to methods of identifying compounds as candidate drugs for treatment of hypoxic conditions and for treating tumors in a subject.
CN101062090A Method for preparing the agent for relieving the pain of cancer patients The invention relates to a preparation for alleviating pains of cancer patients and its preparing process, wherein the constituents include borneol 40-50g, dried alum 10-20g, borax 8-12g, peppermint 10-15g and 95% alcohol 400-500ml.
EP1615611A2 iRNA CONJUGATES Therapeutic iRNA agents and methods of making and using are enclosed.
EP1618880A1 Use of compounds derived from 2,3-dehydronaringenin for the treatment of inflammatory processes and pharmaceutical composition containing said derivatives The present invention refers to the use of 2,3-dehydronarinegenin (apigenin) derivatives of Formula (I) for the treatment or prophylaxis of inflammatory processes and chronic diseases derived from inflammatory processes, as well as to a pharmaceutical composition containing them, together with excipients.
WO2012129957A1 Several pharmaceutical formulations Several pharmaceutical formulations, including pharmaceutical formulation for treating skin roughness, with estrogen as the main component; modified formulation of Huanglian Shangqing tablet for treating cancers, hemiplegia caused by cerebral haemorrhage, psychosis and hemorrhoids; pharmaceutical formulation for treating beriberi, with vitamin C as the main component and with a pharmaceutically acceptable base as an adjuvant to prepare a powder formulation or an aqueous formulation; pharmaceutical formulation for treating common cold, an anti-cold drug is mixed with a pharmaceutically acceptable base, vitamin C for increasing the efficacy against common cold, and other traditional Chinese medicinal herbs to prepare a powder formulation or a tablet formulation.
WO2007057756A3 Isocystene derivatives for the treatment of pain The present invention relates to compounds of formula (I): wherein R1, R2, R4 and R4a are as defined herein. The invention also relates to the use of compounds of formula (I) for the treatment of pain.
CN203417347U Oral microparticle of citrus young fruit extract The utility model relates to an oral microparticle of a citrus young fruit extract. The citrus young fruit extract is used for consuming caloric; the citrus young fruit extract is located in a core layer and at least comprises synephrine, glucose, fat and caloric consumption is promoted, and a metabolic rate is increased; meanwhile, decomposition of a fat cell can be stimulated, so that the efficacy of weight management can be realized; besides, a protection layer is arranged outside the core layer, so that the citrus young fruit extract can be stored and can be effectively absorbed by a human body, and the weight control efficacy is realized to the best.
WO2006023865A1 Oxazolo-naphthyl acids as plaminogen activator inhibtor type-1 (pai-1) modulators useful in the treatment of thrombosis and cardiovascular diseases The present invention relates to oxazolo-naphthyl acids of the formula (I) and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
WO2010096564A4 Dietary supplements containing polyunsaturated omega-3 fatty acids and probiotic bacteria with potential gastrointestinal and dermatological benefits This invention provides a new family of dietary supplements containing polyunsaturated fatty acids, a probiotic culture, and optionally hydrolyzed collagen. The prototype supplement contains cranberry seed oil as a source of omega-3 and omega-6 fatty acids, along with Vitamin E. The prototype supplement also contains a special strain of Lactobacillus casei as well as fish collagen. Nutritional supplements of this invention can be provided in capsule or tablet form, or as a food item such as a chocolate confectionary. Each of the three ingredients confers benefits on their own, allowing the consumer to get three nutritional supplements in the convenience of a single product. The ingredients are also believed to work synergistically to achieve a wider and more durable overall effect. In human clinical trials, consumption of the dietary supplement was associated subjective observations of improvement in softness and moisture of facial skin, reduction in wrinkles, and improvement in function of the gastrointestinal tract.
EP1912641A2 Methods and compositions containing natural folates for protecting against radiation damage Disclosed are methods for protecting a subject from harmful effects of ionizing radiation. The method includes administering to the subject an effective amount of at least one reduced folate. Also disclosed are radioprotective compositions that include a first radioprotective agent and a second radioprotective agent, where the first radioprotective agent is a reduced folate. Methods for protecting a subject from harmful effects of ultraviolet radiation are also disclosed.
CA2659425A1 Triazole compounds that modulate hsp90 activity The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of treating or inhibiting angiogenesis in a subject in need thereof and methods for blocking, occluding, or otherwise disrupting blood flow in neo vasculature, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
WO2006106311A3 Combination treatment methods for treating sex-hormone dependent disease and fertility treatment A method of treating an individual with a condition which condition is one wherein the individual with the condition benefits from the administration of GnRH and/or a GnRH analogue, the method comprising administering to the individual GnRH and/or a GnRH analogue and an inhibitor of prostaglandin synthesis and/or a prostaglandin receptor antagonist. The methods of the invention also include combating a sex-hormone dependent disease in an individual, and regulating fertility in an individual.
CN103202965A Medicine for treating hyperthyroidism and preparation method thereof The invention discloses a medicine for treating hyperthyroidism and a preparation method thereof. The medicine is prepared from the following components according to a certain weight ratio: flos mume, air potato, dens draconis, white hyacinth bean, radices stellariae dichotomae, smoked plum, cortex albiziae and kelp. The medicine has the effects of promoting blood circulation to remove blood stasis, clearing away heat and toxic materials and diminishing swelling and removing stasis, is used for treating hyperthyroidism and is fast in effect, good in curative effect and high in cure rate.
US6946492 Use of C2-substituted indan-1-one systems for preparing medicaments for the treatment of obesity Embodiments of the invention relate to methods of reducing weight in mammals and for the prophylaxis or treatment of obesity comprising administration of C2-substituted indan-1-one systems and their physiologically acceptable salts and physiologically functional derivatives. Compounds for use in methods of embodiments of the invention may include compounds of the formula in which the radicals are as defined, and their physiologically acceptable salts.
USRE41150 Poly(adenosine 5'-diphospho-ribose) polymerase (PARP) inhibitors; compounds based on thieno(4,3,2-ef)(2)benzazepin-6-one This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
US6864247 Therapeutic agents for glomerulosclerosis An object of the present invention is to provide pharmaceutical compositions for inhibiting mesangial cell proliferation or mesangial matrix production without causing hypercalcemia. According to the present invention, therapeutic agents for glomerulosclerosis containing 1α,3β-dihydroxy-20α-(3-hydroxy-3-methylbutyloxy)-9,10-seco-5,7,10 (19)-pregnatriene as an active ingredient are provided.
US6974817 CCR1 receptor antagonists; inhibitors of MIP-1 alpha (CCL3) binding to its receptor CCR1 found on inflammatory and immunomodulatory cells; macrophage inflammatory protein (MIP) A compound of the formula or the pharmaceutically acceptable salt thereof; wherein X, Y, a, b, c, d, R1, R2, R3 and R5 are as defined above useful to treat inflammation and other immune disorders.
CN101810633A Applications of dirithromycin to preparation of medicines for treating chronic noninfective respiratory diseases The invention relates to the field of medicines, particularly discloses application of dirithromycin to the preparation of medicines for treating chronic noninfective respiratory diseases. The chronic noninfective respiratory diseases comprise chronic rhinitis, nose sinusitis, bronchial asthma, chronic obstructive pulmonary diseases, diffuse pan-bronchitis, bronchial cystic fibrosis, bronchitis expansion and occlusive bronchiolitis. The dirithromycin is used for treating chronic noninfective respiratory diseases, can obviously improve subjective symptoms and objective physical signs and has little untoward effect, good patient adaptability and favorable clinical application prospects.
CN101040844A Anticancer compound including alkylate agent and epothilones The invention relates to an anti-cancer compound as a slow release injection which contains alkyl agent and/or aepmycin, formed by slow release micro ball and solvent. The slow release micro ball comprises the anti-cancer effective components and slow release findings, selected from alkyl agent and/or aepmycin, the solvent is a common solvent or a special solvent with suspending agent, while the viscosity of suspending agent is 100cp-3000cp (at 20-30Deg. C), selected from carboxymethyl cellulose, the anti-cancer effective component is phosphoinositide 3-kinase restrainer and/or the phosphoinositide 3-kinase restrainer booster selected from self-anti-cancer antibiotics and/or tetrazine drug, the slow release finding is selected from phosphate polyester as p (LAEG-EOP), p (DAPG-EOP), p (BHET-EOP/TC), p (BHET-EOP/TC), p (BHDPT-EOP/TC), p (BHDPT-EOP/TC), p (CHDM-HOP) or p (CHDM-EOP), or the polyester or mixture of phosphate and polylactic acid, polyphenyl, 2-aliphatic acid, sebacic acid polyester, poly (erucic acid dimmer-sebacic acid) or poly (fumaric acid-sebacic acid). The anti-cancer compound can be made as slow release plant agent, to inject cancer or around cancer to hold the effective drug density for more than 40 days, while it can significantly reduce the general reaction of drug and selectively strengthen the effect of non-surgery treatments as chemotherapy or the like.
US20100160367 Pharmaceutical compositions containing pyrroloquinoline quinone and nephroprotectant for treating ischemia reperfusion injuries The invention includes compositions comprising substantially purified pyrroloquinoline quinone, that are useful in methods for the treatment and prevention of cardiac injury caused by hypoxia or ischemia. The invention also includes methods for the treatment and prevention of cardiac injury comprising contacting a composition of the invention with a human patient.
WO2006097337A2 11β-HYDROXYSTEROID DEHYDROGENASES The present invention relates to novel 11β-HSD inhibitors as well as to the use of 11 β-HSD inhibitors for the manufacture of pharmaceutical agents for the prevention and/or treatment of metabolic diseases, cancer, cell proliferation, glaucoma, diseases associated with abnormal growth hormone secretion as well as wound healing disorders.
CN102757334A Sodium phenylbutyrate type II crystal and preparation method thereof The invention provides a sodium phenylbutyrate type II crystal and a preparation method thereof. The invention further provides a medicinal composition containing the crystal.
WO2006129688A1 2-aminobutanol compound and pharmaceutical use thereof Novel 2-aminobutanol compounds of the following general formula (I) excelling in immunosuppressive action, antirejection activity, etc. and relieved in bradycardia and other side effects, or their pharmaceutically acceptable acid adduct salts; hydrates or solvates thereof; and pharmaceutical compositions comprising these compounds and pharmaceutically acceptable carriers. (I) wherein R is a hydrogen atom or P(=O)(OH)2; R1 is an optionally hydroxylated or halogenated C1-C4 alkyl; R2 is a hydrogen atom or halogen atom or an optionally halogenated C1-C4 alkyl; and R3 is a hydrogen atom or halogen atom or an optionally halogenated C1-C4 alkyl.
CN101161670A Ursolic acid chemical modified compound amine having antitumor activity An amine as a chemical decorative compound with anti-tumor activity is provided, which relates to a natural product and the semi-complex thereof, wherein the present invention carries out chemical decoration for a natural product of ursolic acid to obtain a series of analogs of ursolic acid, i.e., and an amine as a chemical decorative compound with anti-tumor activity. Based on pharmaceutical researches, the amine as the chemical decorative compound of ursolic acid has the significant suppressive activity on Hela cells from Human cervical cancer and SKOV3 cells from ovarian cancer, with advantageous effect on both lines compared with ursolic acid as the parent compound.
US20070027197 Pharmaceutical composition and method for the treatment of diseases using HMG-CoA reductase inhibitors and insulin secretion enhancers or sensitizers The present invention relates to a combination, especially a pharmaceutical composition, comprising as active ingredients (i) a HMG-CoA reductase inhibitor or a or a pharmaceutically acceptable salt thereof; (ii) (a) an insulin secretion enhancer or a pharmaceutically acceptable salt thereof or (b) an insulin sensitizer or a pharmaceutically acceptable salt thereof; and, in case of a pharmaceutical composition, a pharmaceutically acceptable carrier.
US6861417 Such as 2-(4-fluorophenyl)-3-(pyridin-4-yl)pyrazine for treating cytokine mediated diseases such as psoriatic arthritis Novel pyridin-4-yl or pyrimidin-4-yl substituted pyrazine compounds and compositions for use in therapy.
US20120157513 Small Peptide Expression System in Mammalian Cells The present invention is directed to a delivery vector for transferring a small peptide coding sequence to a cell for expression of the small peptide coding sequence within the cell. The delivery vector comprises a secretory signal sequence; a sequence encoding a carrier protein operatively associated with the secretory signal sequence; a sequence encoding a cleavage site operatively associated with the sequence encoding a carrier protein; and a sequence encoding a small peptide operatively associated with the sequence encoding a cleavage site.
WO2009142321A1 Novel thiophenediamine derivative having urea structure The present invention is related to study on synthesis of a novel thiophenediamine derivative having a urea structure and finding of a pharmacological action of the derivative. Specifically, the present invention provides a compound represented by formula (1) or a salt thereof. In the formula, R1 and R2 may be the same or different and each represents a hydrogen atom, an optionally substituted lower alkyl group or the like; R3 represents a hydroxy group, an optionally substituted lower alkoxy group, an optionally substituted lower cycloalkyloxy group or the like; R4 and R5 may be the same or different and each represents a halogen atom, a lower alkyl group, a hydroxy group or the like; X represents an optionally substituted lower alkylene group or the like; Y represents a single bond, an optionally substituted lower alkylene group or the like; W1-W2 represents N-CH, CH-N or the like; and l and m may be the same or different and each represents 0, 1 or the like.
EP2606133A1 Suv420h1 and suv420h2 as target genes for cancer therapy and diagnosis The present invention relates to the roles played by the SUV420H1 and SUV420H2 genes in carcinogenesis and features a method for treating or preventing cancer by administering a double-stranded molecule against the SUV420H1 or SUV420H2 gene or a composition or vector containing such a double-stranded molecule. The present invention also features methods and kits for detecting or diagnosing cancer in a subject, including detecting an expression level of the SUV420H1 or SUV420H2 gene. The present invention further features methods and kits for assessing or determining the prognosis of a subject with cancer, including detecting the expression level of an SUV420H2 gene. Also, disclosed are methods of screening for candidate substances for treating or preventing cancer or inhibiting cancer cell growth, using as an index their effect on the expression or activity of SUV420H1 or SUV420H2.
CN1650848A Clenbuterol hydrochloride inhaling powder mist agent for treating asthma A clenbuterol hydrochloride in the form of inhalant for treating asthma is proportionally prepared from clenbuterol hydrochloride powder and powdered carrier.
CN101601653A Prednicarbate lipidosome cream The invention relates to a lipidosome medical composition which uses prednicarbate as an active component, and a cyst diameter of lipidosome is smaller than 800 nm. The composition comprises 0.025 percent to 0.2 percent of prednicarbate as the active component, 0.5 percent to 6 percent of phospholipid, 0 percent to 1 percent of lipophilic additive, 0.01 percent to 1 percent of antioxidant which is used for preserving the medical composition, a pH buffering agent which is used for retaining the pH value from 5 to 7.5, 3 percent to 15 percent of humectant, 20 percent to 30 percent of oil phrase components, 0.01 percent to 0.1 percent of antimicrobial preservative and the balanced of water. The prednicarbate lipidosome cream is used for treating skin diseases of human beings or animals.
CN1830449A Medical use of flavine-3-beta galactoside and its preparation An medical application of pentahydroxy flavoe-3-beta-galactoside, which can suppress the 3CL proteinase of SARS virus and HcoV-229E antigen-type cold virus, in preparing the medicine for preventing and treating SARS and cold is disclosed. Said medicine is also disclosed.
WO2008074676A1 Pyrazolo [3, 4 -d] pyrimidine p38 map kinase inhibitors Compounds of formula Ia or Ib: wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making 5 the compounds and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases.
CA2125189C Pyropheophorbides and their use in photodynamic therapy Pyropheophorbide compounds are injected into a host and accumulate in tumor tissue to a higher degree than surrounding normal tissues. When the pyropheophorbide compounds are exposed to a particular wavelength of light the compounds become cytotoxic and destroy the tumor or diseased tissue without causing irreversible normal tissue damage. The pyropheophorbide compounds have shown improved results as compared to drugs currently used in photodynamic therapy. Further, they absorb light further in the red, optimizing tissue penetration and are retained in the skin for short time periods relative to other drugs used in photodynamic therapy.
US20110152249 Evaluating central nervous system Evaluating hemodynamic parameters in the cortex can be used as an objective test for CNS activity, e.g., pain.
CN101633660B Novel abietane-type diterpene compound as well as preparation method and application thereof The invention discloses a novel abietane-type diterpene compound as well as a preparation method and an application thereof and relates to the technical field of medicines, in particular to the novel abietane-type diterpene compound which is obtained by separating from Isodonrubescence Hara by certain preparation steps and is named as lushanrubescensin D. The lushanrubescensin D is detected by a plurality of methods, such as a superconducting nuclear magnetic resonance spectrum, a mass spectrum, a Fourier transform infrared spectrum, and the like and is confirmed that the molecular formula thereof is C20H30O3, the molecular weight is 318, and the chemical structural formula is a formula (1). The invention discloses the preparation method, the physicochemical property and the optical activity of the lushanrubescensin D and adopts an MTT method for in-vitro activity screening; and results show that the lushanrubescensin D has obvious inhabitation on mouse sarcoma cells and mouse hepatoma cells, can be used as a lead compound for manufacturing new antineoplastic medicines or can be used as a medicine for treating various clinical familiar frequent cancers.
CA2165995C Medicaments for the treatment of restenosis and arterial sclerosis A medicament for the treatment and/or prophylaxis of restenosis and arterial sclerosis after percutaneous transluminal angioplasty, characterized in that the medicament contains batroxobin as an effective component.
WO2005113569A1 Novel 3-triazolyl-galactoside inhibitors of galectins The present invention relates to novel 3-triazolyl-galactosides, the use of said triazolyl-galactosides as medicament as well as for the manufacture of a medicament for treatment of disorders relating to the binding of galactin to receptors in a mammal. Said galactin is preferably a galactin-3.
CN101784546A Tricyclic heterocyclic compounds as gaba a modulators The invention relates to a compound of the formula (I) with free alkali form or acid addition salt form, its preparation, usage as medicament and medicament comprising the compound, in which R1 represents an optionally substituted aryl group or an optionally substituted heteroaryl group; R2 represents hydrogen or a substituent different from hydrogen; R3 represents an optionally substituted aryl group, cycloalkyl group, heteroaryl group, heterocyclyl group; X1 represents O, S, NR4, CR42; X2 represents O, S, NR4, CR42; X3 represents O, S, NR4, CR42; X4 represents O, S, NR4, CR42; R4 represents hydrogen or substituent different from hydrogen; R5 represents hydrogen or alkyl; Y represents O or S; m represents 0, 1, 2 or 3; and n represents 0, 1, 2 or 3.
US20090054389 Topical Composition Comprising an Antibacterial Substance A pharmaceutical composition for topical application comprises a fusidic acid derivative of general formula I as disclosed herein and one or more monoglycerides of a fatty acid. The composition may be used in the treatment of a disease or condition of the skin or mucosa, in particular skin infections.
WO2010127209A2 Compositions and methods for therapy of macular degeneration Provided are compositions and methods for therapy of macular degeneration including dry age-related macular degeneration (dAMD), juvenile macular degenerations (JMDs) where toxic retinoids are known to accumulate as part of the pathogenesis, such as Stargardt disease, and Best disease, and neovascular wet age-related macular degeneration. The method entails administering to an individual in need of therapy for macular degeneration a first polynucleotide that can facilitate a reduction in the amount of rod opsin (RHO) mRNA in the individual; or a second polynucleotide that can facilitate a reduction in the amount of RPE65 mRNA in the individual; or a combination thereof. The polynucleotides of the invention are hammerhead ribozymes or shRNAs. The polynucleotides target a sequence in RHO mRNA or RPE65 mRNA and facilitate reduction in the target mRNA via ribozymatic cleavage of the target, or by hybridization to the target, which leads to RNAi mediated degradation of the target mRNA.
WO2014083327A1 Adenine derivatives suitable for the treatment of (inter alia) muscular dystrophy The invention provides a compound of formula (I), wherein R1, R2, R3, R4, R5, Ra and Rb have the meanings given in the description, with the proviso that the compound is not a compound selected from the group given in the description. The invention also provides the defined compounds (with or without the proviso) for use in the treatment of muscular dystrophy.
US20110033506 Combination dosage form of low-dose modafinil and low-dose sildenafil Modified release formulations comprising at least one of modafinil and sildenafil, and combinations thereof, and a time-controlled delivery system coating.
WO2010064737A1 Heterocyclic compound and use of the same Provided is a compound represented by general formula (6) and pharmaceutically acceptable salts thereof. (In the formula, R1 is a hydrogen atom or C1-6 alkyl group; R2 is a hydrogen atom or C1-6 alkyl group; R3 is a hydrogen atom, halogen atom, C1-6 alkyl group; or C1-6 haloalkyl group.)
CA2685208C Methods and compositions of inhibiting complement and cellular activation with dextran sulfate A method of inhibiting the adverse effects of complement pathway, activation products in a subject comprising administering to the subject an amount of Dextran Sulfate effective to inhibit formation of alternative complement pathway activation product.
CN101508695A Indolizine-peptide piperazine diketone derivatives, preparation and antimicrobial uses thereof The invention relates to an indolizino phthalazine diketone derivative and a preparation method and antibiotic application thereof. A general structural formula of the compound is shown as formula (I), wherein, R, R and R represent H, R, F, Cl, Br, OH, OR, NH2, NHR, NR'R'', COOH, COOR or aryl, and R, R' and R'' are alkyls; R represents H, R, COOH, COOR, COR, CN or aryl, and R is an alkyl. The preparation method of the compound is simple and easy, and help easily control quality and prepare the compound into medicines in a plurality of forms for use. A medicine consisting of the compound and an adjuvant can obviously inhibit drug resistant Gram-positive bacteria and has low inhibitory activity on nonpathogenic bacteria, which avoids cross infection caused by drug resistant bacteria and provides a treatment means for bacterial infection.
CN101011510A Cervical-lumbar vertebrae pain dispelling liquid Disclosed is a novel medicinal liquid which is prepared from herb of garden balsam 5-7 parts, Sichuan aconite root 3-5 parts, cinnamon 3-5 parts, borneol 11-13 parts, arisaema tuber 4-6 parts, calcined gypsum 4-6 parts, borax 3-5 parts, red peony root 4-6 parts and dahurian angelica root 3-5 parts through ethanol immersion for 40-50 days.
CN102309689A Gastrodia elata chewing gum agent, preparation method and detection method thereof The present invention discloses a gastrodia elata chewing gum agent, a preparation method and a detection method thereof. The gastrodia elata chewing gum agent comprises: 12-20% of gastrodia elata powder, 12-20% of food-grade gum base, 0.5-1% of essence, 20-30% of a wetting agent, 30-50% of a sweeting agent. The gastrodia elata chewing gum agent provided by the present invention has advantages ofrapid onset, easy taking, easy carrying and storing due to small volume, unsusceptibility of microbial contamination due to small water content, xerostomia eliminating, light side effect and good release rate. The preparation method for the gum agent is easy to be operated. The prepared gastrodia elata chewing gum agent with the function of rapid drug release provides good application prospects for treating headache, migraine and other acute diseases. The invention further discloses the detection method for product quality control of the gastrodia elata chewing gum agent.
US20090060883 Composition for promotion of bone growth and maintenance of bone health The present invention relates to a composition for maintenance of bone health or prevention, alleviation and/or treatment of bone disorders. It also relates to the use of the composition in the manufacture of a nutritional product, a supplement, a treat or a medicament; and a method of promoting bone growth or for the maintenance of bone health, which comprises administering an effective amount of the composition.
CA2706505A1 Effervescent compositions The present invention is directed to effervescent compositions comprising a basic amino acid.
CN103211801A Film agent quickly dissolved in oral cavity and preparation method thereof The invention discloses a film agent quickly dissolved in the oral cavity and a preparation method thereof. The film agent consists of the following components in percentage by weight: 0.1 to 70 percent of medicinal active ingredients, 30 to 90 percent of water-soluble film forming material, 2 to 20 percent of plasticizer, 0 to 5 percent of disintegrating agent, and 1 to 20 percent of water, wherein the medicinal active ingredients are selected from modified or non-modified cobra venom, sumatriptan succinate, ergotamine dihydrogen tartrate and lomerizine hydrochloride or flunarizine hydrochloride. The film agent is quick in response, and avoids decomposition in gastrointestinal tracts due to oral administration to reduce the treatment effect. The preparation method is simple, economic and practical, and facilitates industrialized batch production.
US20110217276 Compositions for the prevention and treatment of primary headache and migraine Compositions for the prevention and treatment of primary headache and migraine containing pentacyclic diterpenes obtained from Ginkgo biloba, coenzyme Q10 and Vitamin B2.
US20130035388 Selective inhibition of the membrane attack complex of complement by low molecular weight components of the aurin tricarboxylic acid synthetic complex This patent pertains to selective inhibition of assembly of the membrane attack complex of complement by use of less than 1 kDa molecular weight forms of the aurin tricarboxylic acid synthetic complex (ATAC), and their derivatives. It further pertains to the use of these materials to treat human conditions where there is evidence of self destruction of host tissue by the membrane attack complex. These diseases include, but are not limited to, Alzheimer disease, age related macular degeneration, and atherosclerosis.
WO2011100319A1 Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors The invention provides compounds of Formula (I): that inhibit the PI3Ks and mTOR that are useful in the treatment of cancer in humans when used in combination with autophagy inhibitors.
EP2272835A1 Novel five-membered ring compound Disclosed is a five-membered ring compound represented by formula (1) or a pharmaceutically acceptable salt thereof. The compound inhibits infiltration of leukocytes including eosinophils and lymphocytes, and is effective as a drug for treating various inflammations. The compound is highly safe and can be administered for a long period. A pharmaceutical product containing the five-membered ring compound or a pharmaceutically acceptable salt thereof is also disclosed. (In the formula, R1 represents a halogen atom or a phenyl group which may be substituted by a C1-C3 alkyl group or a C1-C3 alkoxy group; R2 represents a C1-C3 alkylene group which may be substituted by a C1-C3 alkyl group or a carbonyl group; R3 represents a C1-C3 alkyl group; R4 and R5 independently represent a hydrogen atom or a C1-C3 alkyl group, or -N(R4)R5 may represent a morpholino group which may be substituted by a C1-C3 alkyl group; Y2 represents a C2-C4 alkylene group; and R6 represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group or a C1-C3 alkoxy group.)
EP1356812B1 Medicines for treatment and prevention of neurogenic pain Medicines for treatment and/or prevention of neurogenic pain, containing as the active ingredient compounds represented by the general formula (|) or pharmaceutically acceptable salts thereof: (|) wherein R<1> is hydrogen or hydroxyl; R<2> is hydrogen or C1-3 alkyl; R<3> is phenyl which may have one to three substituents selected from the group consisting of halogeno, hydroxyl, C1-3 alkyl, and C1-3 alkoxy, or -NH-R<4> (wherein R<4> is phenyl which may have one to three substituents selected from the group consisting of halogeno, hydroxyl, C1-3 alkyl, and C1-3 alkoxy, or hydrogen); and n is 0 or 1.
CN103690492A Preparation method of lipoic acid particles The invention discloses a preparation method of lipoic acid particles, and belongs to the technical field of preparation of lipoic acid extension products. The preparation method comprises the following steps: weighing anhydrous ethanol and lipoic acid at a weight ratio, putting the anhydrous ethanol and lipoic acid into a stirred vessel, mixing with stirring, then putting the mixture into a sieving device, and sieving so as to obtain lipoic acid thin strips; introducing the lipoic acid thin strips into a shot-blasting machine, performing shot-blasting granulation, and then drying in a drying device to obtain lipoic acid particles non-uniform in particle size; sieving the obtained lipoic acid particles non-uniform in particle size for the first time, and sieving the sieved lipoic acid particles for the second time to obtain the lipoic acid particles uniform in particle size. By adopting the preparation method, the content of lipoic acid in the obtained lipoic acid particles can reach more than 99%, which not only can ensure the safety to human bodies but also is favorable for release and absorption of the lipoic acid particles in the human bodies; the process steps are short and can meet requirements for industrial large-scale production; the obtained particles are uniform in diameter, the density can reach 0.5g/ml, and the particles have good fluidity and are conductive to meeting requirements for preparation production.
WO2009055933A1 Medium-chain length fatty acids and glycerides as nephroprotection agents Use of medium-chain length fatty acids such as capric acid, caprylic acid or lauric acid and their salts or mono- or di- or triglycerides as nephroprotection agents to protect against renal failure progression in chronic kidney diseases This includes the treatment of kidney diseases associated with nephrectomy, renal fibrosis, glomerular scelrosis and end-stage renal disease Also includes the protection of the kidney against cytotoxic agent used in chemotherapy or autoimmune diseases or transplantation Further includes the treatment of renal failure progression associated with hypertension, infarct, tumour, diabetes mellitus, autoimmunity or inflammation.
EP2546253A1 Substituted dihydropyrazolones for the treatment of cardiovascular and hematological diseases Pyrazol-3-one compounds (I) and their salts, solvates and solvate of the salts, are new, where (I) excludes 3-methyl-1-(pyridin-2-yl)-4-(1-pyridin-2-yl-3-methyl-1H-pyrazol-5-yl)-2H-3-pyrazolin-5(1H)-one. Pyrazol-3-one compounds of formula (I) and their salts, solvates and solvate of the salts, are new, where (I) excludes 3-methyl-1-(pyridin-2-yl)-4-(1-pyridin-2-yl-3-methyl-1H-pyrazol-5-yl)-2H-3-pyrazolin-5(1H)-one. R 1>nitrogen containing aryl group of formula (a)-(d); A : C-R 4> or N, where maximum two ring members of A are simultaneously N; E : O, S or N-R 5>; R 2>nitrogen containing heteroaryl-group of formula (e)-(q); a1, a2 : point of attachment with the dihydropyrazolone ring; G : C-R 6> or N, where maximum two ring members of G are simultaneously N; J : O, S or N-R 7>; L : C-R 8> or N, where maximum two ring members of L are simultaneously N; R 4>, R 6>, R 8>H, halo, cyano, NO 2, (1-6C)-alkyl (substituted with 1-3 of T), (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5- or 6-membered heteroaryl (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of T 1>), -C(=O)-R 9>, -C(=O)-R 1> 0>, -C(=O)-NR 1> 1>R 1> 2>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5>, -NR 1> 6>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O)-NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9> or -NR 3> 0>R 3> 1>; T : halo, CN, oxo, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5- or 6-membered heteroaryl, -C(=O)-R 9>, -C(=O)-OR 1> 0>, -C(=O)-NR 1> 1>R 1> 2>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5>, -NR 1> 6>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O) -NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9> or -NR 3> 0>R 3> 1>, where the cycloalkyl-, heterocycloalkyl-, phenyl- and heteroaryl are substituted by 1-3 of halo, CN, (1-4C)-alkyl, trifluoromethyl, OH, (1-4C)-alkoxy, trifluoromethoxy, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl and/or (1-4C)-alkoxycarbonyl; T 1>(1-6C)-alkyl, halo, CN, oxo, -C(=O)-R 9>, -C(=O)-OR 1> 0>, -C(=O)-NR 1> 1>R 1> 2>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5> -NR 1> 6>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O) -NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9> or -NR 3> 0>R 3> 1>, where the alkyl is substituted with 1-3 of halo, CN, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl, (1-4C)-alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5- or 6-membered heteroaryl; either R 9>-R 1> 1>, R 1> 3>, R 1> 4>, R 1> 7>, R 1> 9>, R 2> 1>, R 2> 4>, R 2> 5>, R 2> 6>, R 2> 8>-R 3> 0>H, (1-6C)-alkyl (substituted with 1-3 of halo, cyano, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl, (1-4C) -alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5- or 6-membered heteroaryl), (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of halo, cyano, (1-4C)-alkyl, trifluoromethyl, OH, (1-4C)-alkoxy, trifluoromethoxy, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl or (1-4C)-alkoxycarbonyl); and R 1> 2>, R 1> 5>, R 1> 6>, R 1> 8>, R 2> 0>, R 2> 2>, R 2> 3>, R 2> 7>, R 3> 1>H or (1-6C)-alkyl, which is optionally substituted with halo, CN, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl or (1-4C)-alkoxycarbonyl; or R 1> 1>R 1> 2>, R 1> 4>R 1> 5>, R 1> 6>R 1> 7>, R 1> 8>R 1> 9>, R 2> 0>R 2> 1>, R 2> 1>R 2> 2>, R 2> 3>R 2> 4>, R 2> 6>R 2> 7>, R 3> 0>R 3> 1>5- or 6-membered heterocycloalkyl ring; R 5>, R 7>H, (1-6C)-alkyl (substituted by T), (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl and 5- or 6-membered heteroaryl (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of T 1>); and R 3>H, (1-6C)-alkyl or (3-7C)-cycloalkyl. Independent claims are included for: (1) preparations of (I); and (2) a medicament comprising (I) and inert, non-toxic auxiliary material. [Image] [Image] [Image] [Image] ACTIVITY : Cardiant; Antianemic; Nephrotropic; Antianginal; Cerebroprotective; Vasotropic; Antiarteriosclerotic; Hypotensive; Dermatological; Antimicrobial; Antiinflammatory; Gastrointestinal-Gen; Antiarthritic; Antirheumatic; Ophthalmological; Antiparkinsonian; Neuroprotective; Nootropic; Analgesic; Vulnerary; Anabolic; Endocrine-Gen; Antidiabetic. MECHANISM OF ACTION : Hypoxia-inducible transcription factor (HIF)-prolyl-4-hydroxylase inhibitor.
CN102178688A Preparation method of ivy saponins ingredient and application of the ingredient to resisting tumors This invention relates to a preparation method of an ivy saponins ingredient 3-O-Alpha-L-rhamnopyranosyl-(1-2) (Beta-D-glucopyranosyl-(1-4))-Alpha-L-pyridine Nan ivy saponins arabinose and application of the ingredient to resisting tumors. The invention also relates to application of an extract, which is derived from Pulsatillachinensis (Bunge) Regel rhizome and contains the compound, to resisting the tumors above. The tumors include liver cancer, stomach cancer, glioma, breast cancer, cervical cancer, leukemia, colon cancer, lymphoma and the like.
WO2013177699A1 Inflammation-enabling polypeptides and uses thereof This present technology relates to the use of inflammation-enabling polypeptides (or their coding sequences) to screen for agents useful for the prevention, treatment and/or alleviations of symptoms associated with an inflammatory disorder, to identify individuals susceptible of developing an exacerbated inflammatory response as well as to determine if a therapeutic regimen is capable of preventing, treating or alleviating the symptoms associated to an inflammatory disorder in an individual. The present technology also provides methods for preventing, treating and/or alleviating the symptoms associated to an inflammatory condition based on the inhibition of expression or activity of the inflammation-enabling targets.
US20070298008 Method of bowel cleansing Stimulant laxative in combination with an osmotic laxative produces safe and effective bowel and colon cleansing with a reduced volume of liquid input. Administering to a patient an oral stimulant laxative, such as bisacodyl, followed, after a biologically determined interval, by a reduced volume of a PEG in water solution cleanses the bowels and colon in preparation for diagnostic colonoscopy, without the profuse uncontrollable diarrhea that typically follows either ingestion of large volume isotonic lavages, or smaller volume hypertonic lavages.
CN103183631A Novel isatin-5-sulfonamide derivative and application of same in preparation of medicines used for treating atypical pneumonia The invention relates to a novel isatin-5-sulfonamide derivative as represented by formula I. The formula I is described in the specification; in the formula, R1 is selected from the group consisting of C1-C6 alkyl groups, an aromatic methyl group and a heterocyclic aromatic methyl group, and R2 is a nitrogen-containing heterocyclic group. The invention further relates to a synthetic method for the derivative represented by the formula I and application of the derivative in preparation of medicines used for treating infective atypical pneumonia.
US20050014675 Therapy for vascular system disease; using growth hormonr secretion promoter compound ; artheriosclerosis; cardiovascular disorders; anticholesterol agents An agent for prevention or treatment of vascular disease and renal dysfunction that are accompanied by the migration of vascular smooth muscle cells and mesangial cells comprises as an active ingredient a growth-hormone secretion promoting substance receptor agonist that have a strong inhibitory action on the migration of vascular smooth muscle cells and mesangial cells. Using such an agent for prevention or treatment, one can suppress arteriosclerosis, recurrence of intimal thickening after angioplasty, and even glomerulosclerosis.
WO2006117560A1 Pyrazolyl-amino- substituted pyrimidines and their use in the treatment of cancer This invention relates to novel compounds having the formula (I), and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
WO2014001220A1 Method for prevention of stroke A method for administering Dabigatran, optionally in the form of a pharmaceutically acceptable salt thereof, to a patient in need of an anticoagulant and/or antithrombotic medicament wherein the daily dose is determined by the dosage regimen including one measurement of dabigatran plasma level.
CN1889937B Glycopegylated factor IX The present invention provides conjugates between Factor IX and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue onthe peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates.
EP2291199A2 Capsulating system binding to nucleolin The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.
CN102614140A Iloperidone oral disintegrating tablet and its preparation method The invention relates to a medicinal preparation, concretely relates to an Iloperidone oral disintegrating tablet preparation. The oral disintegrating tablet preparation takes Iloperidone or its medicinal active salt as active components, the prescription ingredients and the weight ratio are as follows: 2-30% of Iloperidone, 40-80% of filler, 1-15% of disintegrating agent, 0-3% of lubricant, 0-3% of flow aid, 0-10% of flavoring agent and 0-20% of adhesive. The invention also provides a preparation method of the oral disintegrating tablet preparation, which comprises the following steps: uniformly mixing the active component raw materials and partial auxiliary materials in the preparation process in advanced, air-flow crushing by controlling the 99% particle size less than 45 micrometers and 90% particle size less than 20 micrometers. The Iloperidone oral disintegrating tablet has the advantages of fast disintegration, rapid dissolution with disintegration time of 2-40 seconds, good mouthfeel, no gritty mouthfeel and high biological availability, and enables compliance of administration requirement of schizophrenia patients, the preparation process is simple, and is suitable for large scale production.
CA2730606A1 Bicyclic heterocycle derivatives and methods of use thereof The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a. G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I)
CN103211755A Production method of sterile stable azithromycin eye drops The invention discloses a production method of sterile stable azithromycin eye drops. The sterile stable azithromycin eye drops comprise a sterile solid drug packaged individually and a special-purpose solvent for dissolving the sterile solid drug. The sterile solid drug contains an active component and pharmaceutically acceptable auxiliary materials. The active component is azithromycin. According to the production method, the active component azithromycin and the pharmaceutically acceptable auxiliary materials are prepared into sterile freeze-dried powder and the sterile freeze-dried powder is dissolved in the special-purpose sterile solvent in clinical use. The production method can improve stability of the azithromycin eye drops, realize production of the sterile stable azithromycin eye drops, and improve safety of the sterile stable azithromycin eye drops in use.
WO2007135427A1 1,4-disubstituted piperazine and 1,4-disubstituted azepane as 11 -beta-hydroxysteroid dehydrogenase 1 inhibitors Compounds of formula (I): wherein variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are described.
US20120148638 Steroid Solavates A dpi formulation comprises a solvate of beclomethasone with a non-cyclic, straight or branched C5-C7 hydrocarbon. The solvate particles are of size 0.5 to 10 microns and are obtained by crystallization of the steroid in the presence of ultrasound.
CN103156865A Application of L-arabinose in preparing medicines or health-care products The invention discloses application of L-arabinose in preparing medicines or health-care products for preventing or treating metabolic syndrome, and in particular application of L-arabinose in preparing medicines or health-care products for simultaneously reducing total cholesterol, triglyceride, fasting blood-glucose, blood pressure, waistline and weight, blood uric acid and glutamic-pyruvic transaminase of human body. The applicant discovers that for adults, in a taking dosage range of 10-20g/person/day, total cholesterol, triglyceride, fasting blood-glucose, blood pressure, waistline and weight, blood uric acid and glutamic-pyruvic transaminase of human body can be simultaneously reduced clinically. Not only is functions of the body not damaged, but also digestion and absorption of proteins and vitamins are not affected while the indexes are simultaneously reduced, so that the purpose of improving the functions of the body and preventing and treating metabolic syndrome is realized.
EP2601940A1 (4-mercapto-piperidin-4-yl)-aminoacetic acid derivatives, pharmaceutical compositions and uses thereof The invention provides (4-mercapto-piperidin-4-yl)-aminoacetic acid derivatives of formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof, for use as a medicament, preferably for use in the treatment and/or prophylaxis of gastrointestinal ulcer, as well as pharmaceutical compositions comprising said thiol derivatives, or a pharmaceutically acceptable salt or stereoisomer thereof, and one or more pharmaceutically acceptable carriers.
US6964783 Non-solid composition for local application The invention concerns a composition, in particular a non-solid pharmaceutical composition for local application comprising, as active principle, at least glycerol or a concentrated solution of glycerol, saccharose, sorbitol or mannitol, the active principle concentration of said composition being osmotically active towards plasma.
CN1559437A Oral Liquid-supplement salt quick-dissolving tablets, prepn. method therefor An orally-applied instant tablet of salt supplementing liquid CRS for supplementing salt to human body is prepared from sodium chloride, sodium citrate, potassium chloride, anhydrous glucose, cane sugar, sorbitol, tween-80, aspartame and PEG300. Its preparing process is also disclosed.
WO2013185294A1 Chinese medicine for preventing and treating rhagades and frostbite and preparation method thereof A Chinese medicine for preventing and treating rhagades and frostbite is prepared by using the following raw materials (parts by weight): ginger (800-1200), cinnamon (40-80), rhubarb (40-80), liquorice (20-60), safflower (80-120), white tuckahoe (50-90), angelica (40-80), scorpion (10-50), clove (10-50), tangerine peel (10-50), medlar (10-50), gleditsia sinensis (50-90), almond (20-60), white mustard seed (5-30), purslane (20-60), pangolin scales (5-40), chicken's gizzard-membrane (10-50), honeysuckle leaves (500-900), astragalus root (260-300), peppermint (5-40), dark plum fruit (2-20), Chinese gall (10-50), calcined dragon bone (5-40), dog bone (5-40), dog oil (10000-14000), camphor (100-500), dragon's blood (5-40), mirabilite (2000-6000), borneol (2-30) and vaseline (2000-6000). The Chinese medicine has the advantages of readily available raw materials and low cost, and provides effects of warming channel for dispelling cold, promoting blood circulation by removing blood stasis, reducing swelling and easing pain and itching, removing necrosis and promoting granulation, avoiding scar formation, beautifying and skin-care.
WO2008084828A1 Method for producing coenzyme q10 particle Disclosed is a method for commercially and efficiently producing a coenzyme Q10 particle having high content and excellent powder flow characteristics by simple facilities and simple operations. Specifically disclosed is a method for producing a coenzyme Q10 particle, which is characterized in that coenzyme Q10 and a poor solvent are stirred and mixed at a temperature not less than the melting point of coenzyme Q10 for dispersing coenzyme Q10 in an oil drop state, and then the thus-obtained dispersion is cooled, while being stirred, to a temperature not more than the solidification temperature of the coenzyme Q10, thereby obtaining solid particles. In this method, the poor solvent is an organic solvent and/or an aqueous solution containing a surface active agent having an HLB of not less than 6. This production method enables to obtain a coenzyme Q10 particle having extremely excellent powder characteristics, for example, a powder flow characteristics index of not less than 80.
CN102716463A Glycyrrhizic acid organic salt phospholipid ligand and preparation thereof The invention relates to a glycyrrhizic acid organic salt phospholipid ligand and a preparation thereof. A new ligand can be obtained by combining organic salt prepared by glycyrrhizic acid with phospholipid, and the obtained ligand can be prepared into oral preparation or injection preparation as required. The base part of the glycyrrhizic acid organic salt can be glycine, methionine, arginine, cysteine, lysine, histidine, glutamic acid, reduced glutathione, methionime, ornithine aspartate or mixtures thereof. The phospholipid is soybean phospholipid, egg yolk lecithin, hydrogenated soybean phospholipid, hydrogenated egg yolk lecithin or polyene phosphatidylcholine. Compositions in the ligand are synergistic, thus the medicament can be well play curative effect and facilitates clinical medicine.
US20080312238 4-Arylazo-3,5-Diamino-Pyrazole Compounds and Use Thereof A series of mono- and binuclear 4-arylazo-3,5-diamino-pyrazoles which are useful for inhibition of cyclin-dependent kinases (preferably CDK9). Hence they can be used as antimitotic-, pro-apoptotic and antiinflammatory drugs, in particular, in chemotherapy of cancer and asthma, therapy of psoriasis and parasitoses as those caused by fungi or protists, treatment of Alzheimer's disease or as anti neurodegenerative drugs, or to suppress immunostimulation. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame-retardants, diagnostic reagents and therapeutics, including antivirals and immunosuppressors.
WO2014093277A1 Xenon and/or argon treatment as an adjunct to psychotherapy for psychiatric disorders The present invention relates generally to the fields of treating psychiatric disorders, in particular, anxiety disorders including post-traumatic stress disorder (PTSD) in subjects, e.g., human subjects, by administering a xenon and/or argon containing composition. Treatments can also employ psychotherapy in combination with administration of xenon and/or argon, alone or in combination with additional psychotherapeutic medications to treat the anxiety disorder and reduce a symptom of the anxiety disorder in the subject.
WO2008148260A1 A novel crystal form of irinotecan hydrochloride and its preparation The invention discloses a novel crystal form of irinotecan hydrochloride which exhibits peaks (2θ) at 7.80°, 9.96°,13.28°,15.62°, 19.98°, 20.36°, 22.34°, 22.66°, 26.60°, 30.18° in powder X-ray diffractometry. Furthermore, the invention also discloses a process for preparing the novel crystal form of irinotecan hydrochloride. Irinotecan hydrochloride obtained by the process according to the invention has good solubility in water, excellent storage stability, high content and purity, and less contaminant.
CN102666490A Aminopyridine compound A compound represented by general formula (I) or a pharmacologically acceptable salt thereof, a medicinal composition comprising the same, and a medicinal composition for the treatment or prevention of respiratory diseases or glaucoma.
CN101199509B Function of 2',2'-CH3-2'H,4H-3,6'-two benzopyran-4-ketone in preparing medicine for treating cancer The invention relates to an application of 2`,2`-dimethyl-2`H, 4H-3, 6`-bis- benzopyran-4-ketone , in particular to an application of the compound 2`,2`-dimethyl-2`H, 4H-3, 6`-bis- benzopyran-4-ketone in preparing drugs for treating related diseases such as estrogen receptor ER-Alpha subtype and ER-Beta subtype, belonging to the medicine field. In the condition of low concentration, the compound does not change the expressions of ER-Alpha66, ER-Alpha46 and ER-Alpha36; while in the condition of high concentration, the compound can inhibit the expressions of the three at the same time. Meanwhile, the compound can kill breast cancer cell MCF7 that expresses the ER-Alpha66, the ER-Alpha46 and the ER-Alpha36. Therefore, the compound can be also used as the regulator of the estrogen receptorER-Alpha36 to treat diseases caused by abnormal expression of the estrogen receptor ER-Alpha36, such as tumor, osteoporosis, asthma, heart disease or senile dementia , etc.
CA2163111C Process for the preparation of an oral solid dosage form containing diclofenac The invention relates to a novel advantageous process for the preparation of an oral solid dosage form containing diclofenac or a pharmaceutically acceptable salt thereof. The dosage form is obtainable by direct compression of an inclusion compound consisting of diclofenac, or a salt thereof, with .gamma.-cyclodextrin. The inclusion compound itself is novel and is likewise an object of the invention.
CA2100329C Methods for treating tumor necrosis factor mediated diseases Methods for treating TNF mediated diseases are provided. The methods comprise administering to patients in need there-of of therapeutically effective amount of a TNF inhibitor. In a preferred embodiment, the TNF inhibitor is selected from the group consisting of 30kDa TNF inhibitor, C105-PEG 3400 db and 40kDa TNF inhibitor, and the 40kDa TNF inhibitor is select-ed from the group consisting of full-length 40kDa TNF inhibitor, 40kDa TNF inhibitor .DELTA.51 and 40kDa TNF inhibitor .DELTA.53. A preferred method for producing the TNF inhibitors is by recombinant DNA technology.
CN102579349A Torasemide liposome injection The invention discloses a torasemide liposome injection. The torasemide liposome injection is prepared from torasemide, cephalin, cholesterol, polyoxyethylene (40) hydrogenated castor oil, one or more antioxidants and one or more protective agents. The torasemide liposome injection has the advantages that preparation stability is good; liposome fracture caused by dehydration and fusion is avoidedin a freeze-drying process; after hydration redissolution, the liposome still retains a good entrapment rate and good stability; and the torasemide liposome injection improves preparation product quality, reduces toxic and side effects of torasemide and is suitable for industrial production.
US6875752 Therapy for grampositive bacteria; bactericides All possible isomeric forms of a compound of the formula where the substituents are defined as in the specification and its non-toxic, pharmaceutically acceptable salts useful as antibiotics.
US6960599 Dopamine D2 receptor and 5-HT1A antagonists; schizophrenia; cognitive activators; Alzheimer's disease; brain disorders; strokes; antiischemic agents; anxiolytic agents; obsessive compulsive disorder; eating, sleeping and sexual disorders The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I: where R1 is the radical of a heterocycle having 1 to 3 ring structures, where each ring structure is saturated, unsaturated or aromatic and optionally fused to other ring structures to give a fused ring system and the heterocycle has a total of 1 to 4 N, O and/or S atoms in the ring structures and is optionally monosubstituted, disubstituted or trisubstituted by one or more of the groups -A, —OR4, —N(R4)2, —NO2, —CN, Hal, —COOR4, —CON(R4)2, —COR4, ═O; R2 is a phenyl group which is optionally monosubstituted, disubstituted, trisubstituted, tetrasubstituted or pentasubstituted by one or more of the groups Hal, -A, —O-A, —NO2 or —CN, or is a thienyl group which is optionally monosubstituted or disubstituted by one or more of the groups Hal, -A, —O-A, -NO2, —CN or thienyl; R3 is H, -A, —CO-A, —C(R4)2R2, —C(R4)2-pyridinediyl-R2; R4 is H or -A; A is C1-C6-alkyl, where 1 to 7 hydrogen atoms are optionally replaced by fluorine; —X— is —O—, —S—, sulfinyl, sulfonyl, —C(R4)2—; —Y— is —[C(R4)2]n—; —Z— is —C(R4)2—; Hal is F, Cl, Br or I; n is 1, 2, 3 or 4; and their tolerable salts and solvates and their use as medicaments.
DE102006005937A1 New fredericamycin derivatives are topoisomerase I inhibitors useful to treat tumor, parasite, immunosupression and neurodermititis Fredericamycin derivatives (I) and their stereoisomers, tautomers and salts are new. Fredericamycin derivatives (I) of formula (Ia) or (Ib) and their stereoisomers, tautomers and salts are new. R1 : H, 1-6C-cycloalkyl, cycloalkyl or 1-4C-alkyl-cycloalkyl; R2 : H, 1-4C-alkyl, 2-14C-alkenyl, (hetero)aryl 1-4C-alkyl-aryl, 1-4C-alkenyl-heteroaryl, (hetero)cycloalkyl, 1-4C-alkyl-cycloalkyl, CmH2m+o-pY1p, (CH2)rCH2NHCOR21, (CH2)rCH2OCOR21, (CH2)rCH2NHCSR21, (CH2)rCH2S(O)nR21, (CH2)rCH2SCOR21, (CH2)rCH2OSO2-R21, (CH2)rCHO, CH2-O-N=CH-(het)aryl, CH2-O-N=CH-R21, CH2-O-N=CR21R22, CH2-O-N=CH=cycloalkyl, CH=N-S-(het)aryl, (CH2)rCH=NOH, (CH2)rCH(OH)R21, (CH2)rCH=NOR21, (CH2)rCH=NOCOR21, (CH2)rCH=NOCH2CONR21R22, (CH2)rCH=NOCH(CH3)CONR21R22, (CH2)rCH=NOC(CH3)2CONR21R22, (CH2)rCH=N-NHCOR23, (CH2)rCH=N-NHC(O)NH-R23, (CH2)rCH=N-NHC(S)NH-R23, (CH2)rCH=N-NHC(NH)NH-R23, (CH2)rCH=N-CH2NHCOR21, (CH2)rCH=N-NHCS-R23, (CH2)rCH=CR24R25 (cis or trans), (CH2)rCOOH, (CH2)rCOOR21, (CH2)rCONR21R22, (CH2)rCH=NR21, hydrazine compound of formula (1), (CH2)rCH=N-NR21R22, (CH2)r-long chain group such as (CH2)rCH=N-N-(1-3C-alkyl-NX1R211R212R213); m : 1-6 (for o is 1, p is 1-2m+o), 2-6 (for o is -1, p is 1-2m+o) or 4-6 (for o is -2, p is 1-2m+o); Y1 : halo, OH, OR21, NH2, NHR21, NR21R22, SH or SR21; X1 : NR215, O or S; R211-R215 : H, 1-6C-alkyl or (CH2)rCH=N-NHSO2-(hetero)aryl; r : 0-5, preferably 0; R21, R22 : 1-14C-alkyl, 1-14C-alkanoyl, 1-6C-alkylhydroxy, 1-8C-alkylamino, 1-6C-alkylamino-1-6C-alkyl, 1-6C-alkylamino-di-1-6C-alkyl, (hetero)cycloalkyl, 1-4C-alkyl-(hetero)cycloalkyl, cycloalkanoyl, 1-4C-alkyanoyl-cycloalkyl, (hetero)cycloalkanoyl, 1-4C-alkanoyl-heterocycloalkyl, 1-4C-alkanoyl-(hetero)aryl or mono-/di- sugar residue (glucuronic acid and its optical stereoisomers C-atom, aldopentose, aldohexose or its deoxy compound such as glucose, deoxyglucose, ribose or deoxyribose), which is linked by C-atom that carries a OH-group; R23 : R21, CH2-pyridinium salt or CH2tri-1-6C-alkylammonium-salt; either R24, R25 : R21, H, CN, COCH3, COOH, COOR21, CONR21R22, NH2 or NHCOR21; or R24+R25 : 4-8C-cyloalkyl; R3 : H, F, Cl, Br, I, OH, OR31, NO2, NH2, NHR31, NR31R32, NHCHO, NHCOR31, NHCOCF3, CH3-mhalm (where hal is Cl or F (preferred) and m is 1-3), OCOR31, SCN, CN, N3, CH2NR331R332, CH2OH, CH2OR33, CH2SR33, 2-14C-alkyl, 2-14C-alkenyl, 2-14C-alkynyl, (hetero)aryl, 1-4C-alkyl-aryl, 1-4C-alkyl-heteroaryl (where (hetero)aryl is substituted with (hetero)aryl, 1-4C-alkyl-(hetero)aryl, O-aryl, 1-4C-alkyl-O-aryl, O-heteroayl or 1-4C-alkyl-O-heteroaryl), (hetero)cycloalkyl, 1-4C-alkyl-(hetero)cycloalkyl, CmH2m+o-pY2p (where m is 2-6 (for o is -1, p is 1-2m+o) or 4-6 (for o is -2, p is 1-2m+o)), CH2NHCOR31, CH2NHCSR31, CH2S(O)nR31 (where n is 0-2), CH2SCOR31, CH2OSO2-R31, CHO, CH=NOH, CH(OH)R31, -CH=NOR31, -CH=NOCOR31, -CH=NOCH2CONR31R32, -CH=NOCH(CH3)CONR31R32, -CH=NOC(CH3)2CONR31R32, -CH=N-NHCO-R33, -CH=N-NHCO-CH2NHCOR31, -CH=N-O-CH2NHCOR31, -CH=N-NHCS-R33, -CH=CR34R35 (trans or cis), COOH, COOR31, CONR31R32, -CH=NR31, -CH=N-NR31R32, hydrazine compound of formula (2), CH=N-NHSO2-aryl, -CH=N-NHSO-2-heteroaryl, SCN, CN, N3, CH2NR331R332 or CH2SR33; X2 : NR315, O or S; R311-R315 : H or 1-6C-alkyl; R331, R332 : R33; Y2 : halo, OH, OR31, NH2, NHR31, NR31R32, SH or SR31; R31, R32 : 1-14C alkyl, 1-14C alkanoyl, 1-6C alkylhydroxy, 1-6C alkylamino, 1-6C alkylamino-1-6C-alkyl, 1-6C-alkylannino-di-1-6C-alk yl, cycloalkyl, 1-4C-alkyl-cycloalkyl, heterocycloalkyl, 1-4C-alkyl-heterocycloalkyl, aryl, aryloyl, 1-4C-alkyl-aryl, heteroaryl, heteroaryloyl, 1-4C alkyl-heteroaryl, cycloalkanoyl, 1-4C alkanoyl-cycloalkyl, heterocycloalkanoyl, 1-4C alkanoyl-heterocycloalkyl, 1-4C-alkanoyl-aryl, 1-4C-alkanoyl-heteroaryl, mono- and di- sugar residues (that are connected over carbon atom, where the sugar carries an OH group and the sugar residues are glucuronic acid and its stereoisomers at all optical carbon atoms, aldopentose, aldohexose including its deoxy compound (like glucose, deoxyglucose, ribose, deoxyribose)); R33 : R31, CH2pyridinium salt or CH2tri-1-6C-alkylammonm
EP1772452A2 Matrix metalloproteinase inhibitors and uses thereof The present invention describes novel compounds comprising: 1-10 targeting moieties; a chelator (Ch); and 0-1 linking groups (Ln) between the targeting moiety and chelator; wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to a cytotoxic radioisotope. The present invention also provides novel compositions of the compounds of the invention, kits, and their uses in treatment of diseases associated with MMPs.
WO2006076277A1 Compositions and methods for increasing the bioavailability of pulmonarily administered insulin A pharmaceutical composition suitable for pulmonary delivery includes insulin and EDTA. The presence of EDTA is effective to increase the relative pulmonary bioavailability of the insulin compared to the relative pulmonary bioavailability exhibited by a composition having the same components but absent the EDTA. The composition is in dry powder form. A method of treating or ameliorating diabetes or a related condition in a mammal includes administering by inhalation a pharmacologically effective amount of the composition. A method of improving the pulmonary bioavailability of an insulin composition includes adding EDTA to an insulin composition suitable for pulmonary delivery, wherein the composition is in dry powder form.
CN103140490A Azaindazole compounds Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR4 or N; and R1, R2, R3, and R4 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
CN102617556A Novel 2-heteroaryl substituted benzothiophenes and benzofuranes 709 The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.
WO2014065439A1 Cancer cell inhibitory drug and cancer stem-cell detection probe An object of the present invention is to provide a cancer cell inhibitory drug, particularly a cancer stem-cell inhibitory drug, or a cancer stem-cell detection probe. The present invention provides a cancer cell inhibitory drug comprising at least one compound represented by general formula (1) as an active ingredient.
US20120225144 Herbal Supplement Prepared From Geranium An extraction method for extracts of Geranium or Pelargonium with improved methylhexaneamine content is provided. The method involves separating the oil phase from the aqueous phase; concentrating the aqueous phase; purifying the oil phase; and recombining the resulting material. Additionally, extracts of Geranium or Pelargonium prepared by the extraction method are provided. The extracts are useful in compositions, for example as dietary supplements, and for appetite suppression.
WO2013124874A3 Glucose derivatives bound to arsenic for use in the treatment of tumour The present invention concerns a family of sugar-based molecules for therapeutic use, comprising compounds with a structure having at least one sugar molecule with carrier function, bound to arsenic having active principle function, allowing the selective therapeutic treatment of tumoral pathologies, distinguished by a high cellular metabolism and, consequently, by a high glucose consumption. Also a process for the production of synthetic sugar-based compounds is the object of the present invention, as well as a process for the production of extracted sugar-based compounds, produced from natural sources. The compounds have the general formula I.
US20080312199 Treatments of therapy resistant diseases and drug combinations for treating the same The present invention provides novel methods and kits for diagnosing the presence of cancer within a patient, and for determining whether a subject who has cancer is susceptible to different types of treatment regimens. The cancers to be tested include, but are not limited to, prostate, breast, lung, gastric, ovarian, bladder, lymphoma, mesothelioma, medullablastoma, glioma, and AML. Identification of therapy-resistant patients early in their treatment regimen can lead to a change in therapy in order to achieve a more successful outcome. One embodiment of the present invention is directed to a method for diagnosing cancer or predicting cancer-therapy outcome by detecting the expression levels of multiple markers in the same cell at the same time, and scoring their expression as being above a certain threshold, wherein the markers are from a particular pathway related to cancer, with the score being indicative or a cancer diagnosis or a prognosis for cancer-therapy failure. This method can be used to diagnose cancer or predict cancer-therapy outcomes for a variety of cancers. The markers can come from any pathway involved in the regulation of cancer, including specifically the PcG pathway and the “stemness” pathway. The markers can be mRNA, microRNA, DNA, or protein.
CN1631385B Ointment for treating burn and scald and its preparing process The invention provides an ointment for treating burn and scald and its preparing process, wherein the ointment is prepared from the following raw materials, shengjun, goldthread root, shiduan, tung seed oil. The ointment has the functions of heat-clearing, detoxifcation, inflammation diminishing, pain reducing, and sterilizing.
WO2011034462A1 Combined anti-tuberculosis preparation The invention relates to medicine and concerns a combined drug having anti-tuberculosis activity in a solid dosage form which comprises, as active principle, a combination of rifampicin, isoniazid, pyrazinamide and a zinc-containing compound, and pharmaceutically acceptable auxiliaries. The claimed composition is characterized by a high level of effectiveness.
CA2551182C Novel kappa receptor selective opioid peptides The present invention provides novel opioid peptides which are selective for the kappa opiate receptor. In one embodiment, the kappa-selective opioid peptides have the general structure Ac-Al-B2-C3-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH2, (SEQID NO. 28), wherein Al is Tyr or Arg, B2 is Arg or Phe, and C3 is Thr, Phe, or Met.In yet other embodiments, the kappa-selective opioid peptides have the general structure (D)Phe-D4-E5-F6 (SEQ ID NO. 29) or (D)Nle-D4-E5-F6 (SEQ ID NO. 30), where in both of these formulae D4 is (D)NapAla or (D)Phe, E5 is (D)Nle, Trp, or (D)Ile, and F6 is (D)Arg or (D)ChAla.
EP1707198A1 Preventive or ameliorating agent for liver disease involving hepatopathy To provide a preventive or ameliorating agent for liver diseases associated with hepatopathy comprising an omega-9 unsaturated fatty acid as an active ingredient.
WO2012121469A1 Antibacterial or preserving composition containing 3-butoxy-1,2-propanediol The present invention relates to an antibacterial and/or preserving composition which contains 3-butoxy-1,2-propanediol as a preserving agent. The antibacterial and/or preserving composition according to the invention has an excellent resistance to microorganisms and has an excellent moisturizing effect, and hardly causes skin trouble.
WO2009001673A1 Atp-containing immunoadjuvant Disclosed are: an immunoadjuvant which has an excellent function of enhancing the production of an antibody and is highly safe; and a vaccine composition comprising the immunoadjuvant. More specifically disclosed are: an immunoadjuvant which comprises ATP or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof as an active ingredient; and a vaccine composition comprising the immunoadjuvant.
EP2283831A2 Biomakers for pre-selection of patients for anti-IGF1R therapy The present invention provides methods for identifying patients whose cancers are likely to be responsive to IGF1R inhibitory anti-cancer therapy along with methods for treating such patients. Patients identified by a method of the present invention can be treated with any of several known IGF1R inhibitory agents including antibodies, small molecule inhibitors and anti-sense nucleic acids.
US20140044753 Composition containing inorganic nanoparticles as an active ingredient for preventing or treating of angiogenesis-related diseases Provided is a pharmaceutical composition containing inorganic nanoparticles selected from titanium oxide nanoparticles or silica nanoparticles as an active ingredient for preventing or treating angiogenesis-related diseases. The pharmaceutical composition for preventing or treating angiogenesis-related diseases according to the present invention may be used as a therapeutic agent for various diseases based on angiogenesis such as age-related macular degeneration, tumors, and diabetes-related complications.
US20100137193 Chitosan derivatives to treat animals or optimize animal health Described herein are methods of inhibiting the growth of or killing a bacterium in an animal subject, preventing or delaying onset of an infection with a bacterium in an animal subject, preventing or delaying onset of a pathogen mediated disease or disorder in an animal subject, or reducing bacterial load in an animal subject, comprising administering an effective amount of a derivatized chitosan to the animal. Also described herein are preparations comprising a chitosan derivative for administration to an animal.
EP1385577B1 Use of nk-1 receptor antagonists against benign prostatic hyperplasia The invention relates to the use of an NK-1 receptor antagonist for the treatment or prevention of benign prostatic hyperplasia (BPH). The preferred NK-1 receptor antagonists are compounds of the general formula (I) wherein the meanings of R, R<1>, R<2>, R<2'>, R<3>, R<4> are explained in the specification and the pharmaceutically acceptable acid addition salts and the prodrugs thereof. Preferred compounds are 2-(3,5-bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide,3-(3,5-bis-trifluoromethyl-phenyl)-N-methyl-N-[6-(4-methyl-piperazin-1-yl)-4-o-tolyl-pyridin-3-yl]-isobutyramide,2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1 lambda <6>-thiomorpholin-4-yl)-4-o-tolyl-pyridin-3-yl]-N-methyl-isobutyramide and 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1 lambda <6>-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide. The invention also relates to pharmaceutical composition comprising one or more such NK-1 receptor antagonists and a pharmaceutically acceptable excipient for the treatment and/or prevention of benign prostatic hyperplasia.
US20100331232 Starch-based hydrogel for biomedical applications A starch-based hydrogel for the controlled delivery of a biologically active agent is described. The hydrogel comprises a dispersed phase, and a dispersion medium consisting substantially of water. The dispersed phase includes a polymeric network comprising a hydrolyzable polymeric substance derived from starch, and a cross-linker. In various embodiments, the polymeric starch-derived network includes amylose, amylopectin, or a combination thereof, or soluble starch. The cross-linker is a molecule having at least two carboxyl moieties. The hyrogel is biocompatible and biodegradable, and suitable for loading with biologically active agents ranging from small molecule therapeutics to macromolecules such as proteins, polysaccharides and nucleic acids. Upon administration to a host animal, the hydrogel biodegrades, releasing as degradation products only naturally-occurring sugar molecules that are non-toxic and non-immunogenic to the host.
CN101580497A Statins antilipemic drugs furazan nitroxides derivates and preparation method thereof The invention relates to a statins antilipemic drugs furazan nitroxides derivates and a preparation method thereof, and solves the problems of nonlipid-lowering and low activity in statins antilipemic drugs and adverse effect. The invention is shown as formula (1).
CN103119028A 1,2,4-Triazolone Derivative The present invention provides a 1,2,4-triazolone derivative represented by general formula (1A), which acts as an arginine vasopressin 1b receptor antagonist; a pharmacologically acceptable salt thereof; and a drug containing the same as an active ingredient, particularly a therapeutic or prophylactic agent exhibiting favorable in-vivo disposition in the case of mood disorders, anxiety disorders, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorders, hypertension, gastrointestinal disorders, drug dependency, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head trauma, inflammation, immunological disorders, hair loss, and other diseases.
CN102920690A Chemical medicine for treating cerebral-cardio vascular diseases The invention discloses a chemical medicine for treating cerebral-cardio vascular diseases. The chemical medicine is characterized in that the chemical medicine comprises the following raw materials, by weight, 1 part of potassium dihydroxybenzenesulfonate, 0.05-50 parts of an excipient, 0.001-0.05 parts of an antioxidant, and 0.001-0.02 parts of a metal chelating agent. The chemical medicine has the advantages of simple technology, high yield, low production cost and high stability, can obviously improve the microcirculation, and has obvious advantages in the treatment of the cerebral-cardio vascular diseases.
CN101820880A Therapeutic agent for inflammatory bowel disease comprising uracil derivative as active ingredient Disclosed is a therapeutic agent for inflammatory bowel disease. Specifically disclosed is a therapeutic agent for inflammatory bowel disease, which comprises a uracil derivative represented by the general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient.
US20080280944 Sleep disorders; administering a potassium channel moderator The present invention relates to a new method of treatment of sleep disturbance due to silent gastro-esophageal reflux. In particular, the present invention relates to the use of certain imidazo (1,2-a)pyridines derivatives (I) in said treatment.
CN1600788A Distinguishing gene for adjusting and controlling anti-oncogene p53 and usage In the invention, a new gene with kinase activity related to cancer suppressing gene is found. It is confirmed by experiment that said gene and coded protein have extensive uses in way of participating activity of cancer suppressing gene, preparing tumour preventive treating medicine and diagnosing reagent etc.
WO2008084496A1 Novel substituted 1h-benz [de] isoquinoline-1, 3 -diones The present invention relates to novel substituted 1H-benz[de]isoquinoline-1,3-diones. This invention particularly relates to novel substituted 1H-benz[de]isoquinoline-1,3-diones particularly N-[2-(Chloroethyl)]- and N-[3-(Chloropropyl)]-naphthalimides and antitumor activity thereof. The present invention also relates to process of preparation of novel substituted 1H-benz[de]isoquinoline-1,3-diones. The present invention further relates to pharmaceutical composition for the treatment of cancer and related diseases.
CN1834108B Acanthopanax giraldii Harms compound polysaccharide, preparation technique, uses and its compound polysaccharide composition This invention relates to a kind of composite polysaccharide that is extracted, separated and purified from the stem skin of acanthopanax giraldii harms, has a weight-average molecular weight of 20000~40000 and mainly comprises Arabinogalactan proteins (AGPs), Rhamnogalacturonan Is (RGI), Homogalacturonans (HGs) and Arabinogalactans (AGs). A proper amount of acanthopanax giraldii harms composite polysaccharide is taken and one or more species of pharmacologically permitted agent are added to produce injections. Each injection unit contains at least 30mg of the substance in this invention. It is applicable in the therapy of neutropenia, anemia, pancytopenia and virus-infected diseases and can be used as anti-cancer agent. It can be taken independently or coupled with other polysaccharides or G-CSF.
CN103127077A Application of Aphanamixoid A to dental ulcer treatment or prevention medicine The invention relates to application of Aphanamixoid A to preparation of dental ulcer treatment or prevention medicine. The application of the Aphanamixoid A to the preparation of the dental ulcer treatment or prevention medicine is made public for the first time. The skeleton type is fully novel, activity of the Aphanamixoid A in treating dental ulcer is surprisingly strong, the possibility that inspiration is obtained from other compounds does not exist, the Aphanamixoid A has prominent substantive features, and meanwhile, significant progress of the application of the Aphanamixoid A to treatment of the dental ulcer is obviously achieved.
EP1531873A2 Agent delivery particle A composition comprising a substantially spherical polymer particle having a diameter of about 1200 microns or less. The agents can be radioactive species. The agents can be therapeutic agents. The agents can be in and/or on the particles.
CN101094839A Quinazoline derivatives, process for their preparation, their use as antimitotics and pharmaceutical compositions comprising said derivatives The invention relates to quinazoline derivatives of formula (I), in which R<1>, X and A have the meanings as indicated, or to a pharmaceutically acceptable salt thereof, e.g. (formula II). Such compounds are useful as modulators, in particular inhibitors, of the mitotic kinesin Eg5. i.e. the human protein (also called KSP), the Xenopus laevis homologue, further homologues from other species as well as allelic variants and functionally related proteins. The invention also relates to processes for their preparation, pharmaceutical compositions comprising said quinazoline derivatives, and the use of said quinazoline derivatives, in particular for treating diseases such as cancer.
EP1718299A1 Heterocyclic gaba-a subtype selective receptor modulators This invention relates to the use of compounds of formula (I) for the manufacture of a medicament useful for modulating α2 subtype GABAA receptors. The invention further relates to novel heteocyclic compounds and pharmaceutical compositions containing said compounds. In addition the invention relates to the treatment of depression, an anxiety disorder, a psychiatric disorder, a learning or cognitive disorder, a sleep disorder, a convulsive or seizure disorder or pain.
CN101564496B Plaster for mainly curing periarthritis of shoulder The invention provides a plaster for mainly curing osteoarthropathy and soft tissue injury. The plaster is prepared by balm as an auxiliary material and other raw material medicines as active ingredients, such as turtle shells, sepium, Chinese honey locust, Bletilla striata, frankincense, myrrh, dragon's blood, red paeonia, hemlock parsley, angelica, and the like. The plaster activates blood circulation to dissipate blood stasis, expels wind to relax vein, removes rotten to let fresh grow, frees numb, removes damp, clears heat, purges fire, induces sensation, removes food retention, effectively improves the effects of curing the osteoarthropathy and the soft tissue injury, is convenient to cure while relieving the pain of patients and can be also used for curing gastric satiety, gastrectasia, gastricism, gastric ulcer, chronic enteritis, kidney stone, prostatosis, stasis-type coronary heart disease, dysmenorrheal, lobular hyperplasia of mammary gland, and the like with favorable curative effects.
WO2014022748A1 The use of antithrombin in extracorporeal membrane oxygenation In one aspect, the disclosure provides methods of suppressing blood clotting and/or preventing hemorrhage in a subject having extracorporeal membrane oxygenation comprising administering antithrombin. In some embodiments, the antithrombin used in the methods disclosed herein is ATryn®.
CN101884623A Levodopa methyl ester slow-release microsphere composition and preparation method thereof The invention relates to a levodopa methyl ester slow-release microsphere composition, which consists of the following components in percentage by weight: 50 to 99 percent of degradable hydrophobic polymer, and 1 to 50 percent of levodopa methyl ester. The invention also provides a preparation method of the levodopa methyl ester slow-release microsphere composition. The levodopa methyl ester slow-release microsphere composition overcomes the problems that the current oral dosage regimen is single, frequent oral administrations are required, frequent missed administrations are caused to patients of the type, and an effective treatment cannot be achieved; and the preparation method using one type of W/O/W is provided. The grain size of the levodopa methyl ester slow-release microsphere composition can be controlled according to different needs, and the levodopa methyl ester slow-release microsphere composition cannot pollute the environment; and influences on the curative effect of the levodopa methyl ester can be avoided. The grain size can be adjusted and controlled from 1 mu m to 500 mu m according to needs; and freeze-dried powder of the levodopa methyl ester slow-release microsphere composition is white, subtle and loosened, cannot collapse and adhere together, and has high redispersibility. Compared with an oral preparation with the same dosage, the effect of the levodopa methyl ester slow-release microsphere composition is obviously better than that of the oral preparation.
CN101972460B Composition for treating beriberi and preparation method thereof The invention relates to a composition for treating beriberi. The composition is prepared from the following raw materials: vinegar, ginger, potassium permanganate, table salt and 1 percent medical iodophor. A preparation method of the composition comprises the following steps of: crushing the ginger into fine powder in a crusher; putting the vinegar, the ginger fine powder, the potassium permanganate, the table salt and the 1 percent medical iodophor according to a weight ratio into a stirrer, and stirring and mixing the mixture for 10 to 30 minute; inspecting degree of uniformity; and packing a product with bottles or plastic bags according to a unit of 100g or 200g or 300g or 500g by weight to obtain the composition for treating the beriberi. The composition for treating the beriberi has the effects of diminishing inflammation, sterilizing, dissipating cold and eliminating dampness, and has obvious effects of treating the beriberi, decontaminating, moisturizing skin, deodorizing and resisting fungus. The composition not only improves the quality of feet washing and removes skin dirt of feet, but also has the effects of relieving rigidity of muscles and activating blood, promoting blood circulation, enhancing metabolism, preventing and treating diseases and caring health and strengthening physical health if being frequently used.
CN1803150A Method for obtaining binded estrogen mixture from pregnant horse urine, and its uses of big pore adsorption resin in the method The invention discloses an estrogen mixture acquisition method from pregnant horse urine and appliance of big-hole adsorption resin, which comprises the following steps: predisposing the raw material of pregnant horse urine; adsorbing the bond estrogen mixture in the pregnant horse urine through big-hole adsorption resin; cleaning the big-hole adsorption resin of negative load bond estrogen mixture through alkaline aqueous solution; eluting the big-hole adsorption resin to obtain the bond estrogen mixture. The big-hole adsorption resin adapts phenylethene-diphenyl ethylene middle polarity resin with ester group structure. The invention improves the extraction efficiency and reduces the extraction cost, which is fit for large-scale production.
WO2014075394A1 Novel gold(iii) complexes containing n-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growthin vivo.
CN1565437A Verapamil hydrochloric acid drop pill and its preparation method The invention relates to dripping pills of verapamil hydrochloride and its preparation by using hydrochloric verapamil as the principal raw material andding base material such as polyethylene glycol as surface active agent, mixing evenly, and dropping into condensation agent for cooling down.
US20060069084 Methods of inhibiting kinases The present invention provides methods of inhibiting JAK involving the use of a group of compounds based either upon a 2-amino-6-carba-disubstituted pyrazine scaffold or a 2-amino-6-carba-disubstituted pyridine scaffold. The invention also provides methods of treating JAK-associated disease states.
CN103130793A 3-(1-aryl-piperidin-4-yl)-2-aryl-thiazole-4-ketone compound, preparation method thereof and use thereof The invention belongs to the field of pharmaceutical chemicals, and relates to a 3-(1-aryl-piperidin-4-yl)-2-aryl-thiazole-4-ketone compound, medicinal salt thereof, a preparation method thereof and use thereof, in particular to a compound shown in the formula I or medicinal salt thereof. The 3-(1-aryl-piperidin-4-yl)-2-aryl-thiazole-4-ketone compound or the medicinal salt thereof has obvious N-type calcium channel blocking-up activity and good pharmacokinetics properties, can prevent and cure or relieve pain effectively, and has potential used as novel medicine for preventing and/or treating pain, apoplexy and cerebral ischemia, alcohol addiction and intoxication, acute and chronic renal failure, or renal insufficiency.
US7875728 Hydrazonopyrazole derivatives and their use as therapeutics Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
WO2014070760A1 Use of resazurin, or analogs thereof, for antibacterial therapy A method for treating infection by bacteria in a subject, comprising administering to the subject a therapeutically effective amount of resazurin or a resazurin analog, or a pharmaceutically acceptable salt or ester thereof, wherein the bacteria is selected from at least one of Francisella sp. or Neisseria sp.
US20080267996 Compositions for inducing an immune response against hepatitis B The present invention is directed to a method of inducing an immune response against a hepatitis B antigen (e.g., an antigen from a hepatitis B virus) in a mammal, which comprises administering to the mammal a priming composition (e.g., a DNA plasmid), comprising a source of one or more epitopes of the hepatitis B target antigen; and a boosting composition, comprising a source of one or more eptiopes of the hepatitis B target antigen (e.g., a non-replication or replication-impaired poxvirus such as MVA), wherein at least one epitope of the boosting composition is identical to an epitope of the priming composition. The present invention also is directed to a method of inducing an immune response against a hepatitis B antigen (e.g., an antigen from a hepatitis B virus) in a mammal, which comprises administering to the mammal a priming composition (e.g., a DNA plasmid), comprising a source of one or more epitopes of the hepatitis B target antigen. In addition, the present invention is directed to compositions for use in the methods of the present invention.
US6906085 Tetrahydropyran derivatives as neurokinin receptor antagonists The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7 and R8 represent a variety of substituents; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
CN102793658A Matrix-type preparation containing mycophenolic acid or mycophenolic acid salt and coated tablet thereof The invention discloses a matrix-type preparation containing mycophenolic acid or a mycophenolic acid salt and a coated tablet thereof, and belongs to the technical field of medicinal preparations. The matrix-type preparation and the coated tablet thereof contain mycophenolic acid or a mycophenolic acid salt, and one or more pharmaceutically acceptable enteric polymers, one or more filling agents, one or more disintegrating agents and one or more lubricants and/or one or more adhesives. The matrix-type preparation containing mycophenolic acid or a mycophenolic acid salt and the coated tablet thereof can convey a drug to an upper end of the intestinal tract and release the drug so that precipitation of the drug in the stomach is avoided and bioavailability is improved.
WO2010136846A1 Differentiation therapy for sarcomas Use of muscle-enriched/specific microRNAs for the treatment of sarcomas, as for example rhabdomyosarcomas, synovial sarcoma, alveolar soft part sarcoma, liposarcoma, and osteosarcoma, wherein the microRNAs are able to stop the development of neoplastic cells and to force the neoplastic cells to differentiate into terminally differentiated muscle cells.
WO2011098456A1 Safinamide in the treatment of dyskinesia The present invention relates to the treatment and prophylaxis of dyskinesias, preferably dyskinesias associated with dopaminergic therapy.
CN102159547A Heterocyclic carboxamide compounds This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
US20090012021 Delivery of Sirna by Neutral Lipid Compositions The present invention relates to the fields of molecular biology and drug delivery. In certain embodiments, the present invention provides methods for the delivery of a siNA (e.g., a siRNA) to a cell via a neutral (non-charged) liposome. These methods may be used to treat a disease, such as cancer.
WO2010044681A1 A medicinal product and treatment The use of paracetamol and ibuprofen in the preparation of a medicament for treating osteoarthritis or rheumatoid arthritis, wherein the medicament comprises a combination composition having approximately 125 mg to approximately 150 mg ibuprofen and approximately 475 mg to approximately 500 mg paracetamol.
WO2008141843A1 Novel sulphoximine-substituted quinazoline and quinazoline derivatives as kinase inhibitors The present invention relates to a quinoline or quinazoline derivative having the general formula (A): in which R3, R4, W, Y and Q are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).
US20130045249 Glycosaminoglycans Heparan sulphate HS/BMP2 is disclosed, together with the use of HS/BMP2 in the repair and regeneration of bone tissue.
US20120309730 Oxysterols that activate liver x receptor signaling and inhibit hedgehog signaling This invention relates, e.g., to compositions comprising oxysterol compounds represented by Formula I or Formula II, e.g., comprising one or more of Oxy 16, Oxy 22, Oxy30, Oxy 31, Oxy35, Oxy37, Oxy43, Oxy44, Oxy45 or Oxy47. The compounds are shown to be Hedgehog pathway inhibiting, and to act as agonists for liver X receptor (LXR). Also disclosed are methods of using compositions of the invention to inhibit Hedgehog signaling effects, such as cell proliferation, including treating subjects in need thereof, and pharmaceutical compositions and kits for implementing methods of the invention.
CN103405446A Application of Chukrasone A in medicaments for treating bile duct carcinoma The invention discloses an application of Chukrasone A in preparing medicaments for treating bile duct carcinoma, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluation finds that the Chukrasone A also has a significant inhibitory effect on the growth of human bile duct carcinoma cell strains RBE. Therefore, the Chukrasone A can be used for preparing anti-bile duct carcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating human bile duct carcinoma provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to human bile duct carcinoma cells.
US20100074851 Cosmetic or pharmaceutical composition containing hyaluronic acid A cosmetic or pharmaceutical composition includes particles of hyaluronic acid having a molecular weight between 20000 Da and 3000000 Da, combined with a polyamine.
CN1872076B Drop pills of cucurbitacine, and preparation method A dripping pill of cucurbitacin for treating chronic metastatic hepatitis features high natural level and safety and low toxic by-effect. Its preparing process is also disclosed.
WO2009076473A1 2-{[2-(substituted amino)ethyl]sulfonyl}ethyl n,n-bis(2- chloroethyl)phosphorodiamidates 2- {[2 (Substituted amino)ethyl]sulfonyl}ethyl N,N bis(2 chloroethyl)phosphorodiamidates and their salts, their preparation and intermediates in their preparation, pharmaceutical compositions containing them, and methods of treatment using them. The compounds are useful for treating cancer and autoimmune diseases, alone and in combination with other therapies.
EP2342185A1 Sulfone-substituted anilinopyrimidine derivatives as cdk inhibitors, the production thereof, and use as a medicine The invention relates to sulfone-substituted anilinopyrimidine derivatives of formula (I), to a method for producing the same, and to the use thereof as a medication for treating various illnesses.
US20120316135 Compounds for Inhibiting Cell Proliferation in EGFR-Driven Cancers The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.
CN102114042A Intestinal tract cleaning solution specially used for preoperation of children with hirschsprung disease The invention belongs to the technical field of medicines and discloses an intestinal tract cleaning solution specially used for preoperation of children with hirschsprung disease. The cleaning solution is prepared by using saxoline, 50% magnesium sulfate, hydrogen peroxide, gentamicin and physiological saline as raw materials, respectively proportioning the raw materials according to different characteristics of each medicinal raw material, uniformly blending, separately filling by 100ml/bottle, sealing, sterilizing, and labeling to obtain the cleaning solution. The cleaning solution can fully clean the intestinal tract, greatly shorten the preparation time before the operation of the children with hirschsprung disease, and simultaneously shorten the hospital stays and relieve the family burden of the children with hirschsprung disease. By using the cleaning solution, the physiological saline required for coloclysis in each time can be reduced, the time for coloclysis in each time can be shortened, the mental and physical pain of the children with hirschsprung disease can be relieved, the body consumption of the children with hirschsprung disease can be reduced, and the tolerance to the operation can be improved. The cleaning solution has the advantages of promoting colitis diseases to subside quickly, preventing colitis after the operation, and the like. The intestinal tract cleaning solution disclosed by the invention also has the advantages of simpleness of preparation, convenience for operation, low cost, and easy acceptability to patients. As proved by 120 cases of children with dental ulcer in clinic, the total effective rate of the intestinal tract cleaning solution disclosed by the invention reaches 96%, and no special toxic or side effect is found.
CN102379841A Preparation method of furacilin solution The invention discloses a preparation method of a furacilin solution, and the product belongs to the field of pharmacy. The furacilin solution is an external local antibiotic medicine which is commonly used clinically in hospitals in China, is the yellow clear and transparent liquid in appearance, has slight bitter taste, and has the functions of interfering the sugar metabolic process and the oxidase system of bacteria, and accordingly, the bacteriostatic or bactericidal purpose is realized. The product is produced from the raw materials of: furacilin powder, officinal sodium chloride, analytically pure sodium benzoate, polysorbate, officinal diluted hydrochloric acid and distilled water. The product adopts the improved method to produce the furacilin solution, and the method has simple technology, high product concentration, good bactericidal effects and good stability.
US20070066590 Phenyl-and pyridylpiperidine-derivatives as modulators of glucose metabolism The present invention relates to certain substituted aryl and heteroaryl derivatives as shown in Formula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.
WO2008098122A2 Method for treating allergic rhinitis without adverse effects The present invention is directed to a method for treating allergic rhinitis without causing an adverse effect of bitter taste. The method comprises administering to a patient an aqueous pharmaceutical formulation comprising 0.1- 0.15% (w/v) of epinastine or an acid addition salt thereof, 0.05 -0.5% (w/v) of hydroxypropylmethylcellulose to maintain the viscosity between 1.5-10 centipoise, 1-2% (w/v) of propylene glycol, and a buffer to maintain the pH between 5-8, said aqueous epinastine formulation has a tonicity between 200-400 mOsm/kG; the formulation does not contain a significant amount of a sweetening agent. The present invention provides a method for effectively treating allergic rhinitis by delivering a small volume of the epinastine formulation to the nose of a patient using a small volume metered-dose nasal spray pump. The present method does not cause an adverse effect of bitter taste without including sweetening agents in the formulation.
WO2006123244A2 Carbamate derivatives as positive allosteric modulators of metabotropic glutamate receptors The present invention relates to new compounds which are Carbamate derivatives of formula I wherein X, B, P, Q5W, R1 and R2 are defined in the description. Invention compounds are useful for treating CNS or PNS disorders which are affected by the neuromodulatory effect of mGluR5 positive allosteric modulators such as cognitive decline and also to treat both positive and negative symptoms in schizophrenia
EP1598063A1 Synergic compositions comprising vitamins, minerals and trace elements to stimulate removal of intracellular lipids An oral synergistic composition (A) is used for reducing the accumulation of intracellular lipids. (A) contains at least two vitamins and at least two minerals or trace elements to treat excessive body weight. - ACTIVITY - Anorectic. - MECHANISM OF ACTION - Elimination of intracellular lipids from adipocytes.
WO2014039001A1 Tiotropium preparations The present invention relates methods of preparing particles of tiotropium bromide particularly useful for inhalationdelivery, the particles obtained from such methods, and their use in pharmaceutical compositions for treatment of respiratory disorders, such as COPD (chronic obstructive pulmonary disease) and asthma.
EP1923055A1 Freeze-dried pharmaceutical composition comprising an S1P agonist or modulator The present invention provides a rapid disintegrating pharmaceutical composition comprising a freeze dried dosage form of an S1P agonist or modulator.
US7504433 e.g. (2-Methyl-4-{2-[3-methyl-5-(4-trifluoromethyl-phenyl)-thiophen-2-yl]-propylsulfanyl}-phenoxy)-acetic acid;peroximose proliferator activated receptor; antidiabetic agent,atherosclerosis The present invention is directed to compounds represented by the following structural formula, Formula I: and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) X is selected from the group consisting of O, S, S(O)2, N, and a bond; (b) U is an aliphatic linker wherein one carbon atom of the aliphatic linker may be replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with R30; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; and (d) E is C(R3)(R4)A or A.
CN103239471A External preparation for skin moistening The invention relates to an external preparation for skin moistening. The preparation is formed by an effective component and medically acceptable auxiliary materials, and is characterized in that the effective component is dendrobium officinale polysaccharide with the molecular weight of 85-90 KDa. The external preparation for skin moistening disclosed by the invention can increase the expression quantity of a skin aquaporins-3 gene so as to accelerate further multiplication of malpighian cells and obviously improve a skin water retention effect.
US20100280003 Combinations of jak inhibitors The invention provides a pharmaceutical combination comprising: a) at least one agent selected from Bcr-Abl, Flt-3, FAK and RAF kinase inhibitors; and b) at least one JAK kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.
US20120083447 Novel Therapeutic Treatments Using Centhaquin Methods of treating hypertension, pain, and resuscitative hemorrhagic shock using an adrenergic agent, like centhaquin, are disclosed. The methods treat mammals, including humans.
CN1586481A Procaterol dripping pill and its preparing method The present invention relates to procaterol preparation, and especially one new kind of procaterol dripping pill for treating bronchial asthma, asthma bronchitis and chronic obstructive lung diseases and its preparation process. The medicine releasing rate of procaterol may be regulated via selecting different dripping pill matrix, composition and coating material. The preparation may contain stabilizer and corrective, the dripping pill may have or have no coating, and the dripping pill may be held under tongue or orally taken with completely dissolving and dispersing time of 1-15 min. The present invention has simple preparation process, controllable quality, high stability and convenient use.
WO2011159065A2 Method for preparing medicinal herbs used in treatment of malignant swelling The present invention relates to a method for preparing medicinal herbs used in the treatment of malignant swelling, comprising: the first step of spreading 3cm or more of ocher soil on the bottom of a manufacturing container in the shape of an iron pot; the second step of spreading medicinal herbs comprising a first material comprising Populus diversifolia, myrrh and frankincense, a second material comprising orpiment and any one mineral selected from tansonic stone, Arsenolite, realgar or soil stone, a third material comprising musk and ox bezoar, a fourth material comprising natural Cinnabaris and cinnabar, and a fifth material comprising vermiculite, on the ocher soil spread on the bottom of the manufacturing container; the third step of covering the opened upper portion of the manufacturing container with a lid of the manufacturing container in the shape of a saucepan lid; the fourth step of covering the lateral side of the lid of the manufacturing container and the outer part of the region in which the manufacturing container comes in contact with the lid, by using a material comprising cheonilam and clay; the fifth step of continuously heating the manufacturing container for 48 hours or more; and the sixth step of continuously dropping a predetermined amount of cold water onto the upper portion of the lid of the manufacturing container during the heating of the manufacturing container in the fifth step, wherein the material attached to the lower portion of the lid of the manufacturing container is collected after completion of all the steps and is used as a medicinal herb material used for treating malignant swelling.
US20120252745 Novobiocin analogues having modified sugar moieties The disclosure provides novobiocin analogues with noviose replacements which are useful as Hsp90 inhibitors in the treatment of cancer.
CA2205406C Novel benzyl pyrimidines Substituted 5-benzyl-2,4-diaminopyrimidines of general formula (I) in which R1 represents lower alkoxy, R2 represents bromine or lower alkoxy and R3 represents aryl, heteroaryl or a group -Q-R30, wherein Q signifies ethylene, vinylene or ethynylene and R30 signifies aryl, heteroaryl, lower alkoxy-carbonyl or carbamoyl, as well as readily hydrolyzable esters of carboxylic acids of formula I and pharmaceutically acceptable salts of these compounds can be used in the control or prevention of infectious diseases.
CN101766579A Duloxetine enteric-coated sustained release preparation as well as core material and preparation method thereof The invention discloses a Duloxetine nteric-coated sustained release preparation as well as a core material and a preparation method thereof. The core material consists of Duloxetine as active medicinal ingredient or salts thereof and pharmaceutically acceptable auxiliary, wherein the pharmaceutically acceptable auxiliary contains a hot-melt material which at least contains a water-soluble hot-melt material and a hydrophobic hot-melt material, and the content of the hot-melt material is 20%-35%, the content of Duloxetine or salts thereof is 50%-75%, the rest is other pharmaceutically acceptable auxiliary the percentage of which is the mass percentage thereof based on the total amount of the core material. According to the invention, the core material of the Duloxetine nteric-coated sustained release preparation is prepared by adopting hot-melt technology, which avoids the introduction of water or organic solvents during preparation, lessens the degradation of principal and residual solvent, achieves a proper delay on the release of Duloxetine in intestines, namely 4-hour release amount in phosphate buffer with 6.8 of pH accounting for over 70% of the total amount, and is favorable for reducing adverse reaction of patients.
WO2008029876A1 Salt of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1- methylpyridin-2(1h)-one and crystal thereof A salt of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1- methylpyridin-2(1H)-one, and a crystal thereof.
CA2597812C Parenteral combination therapy for infective conditions with drug resistant bacterium The invention describes a pharmaceutical composition to combat multiple-drug-resistant bacteria in non-ocular infective conditions. Compositions comprising glycopeptides, in particular vancomycin, and cephalosporins, in particular ceftriaxone, are disclosed. Such compositions are found to be useful for parenteral administration for hospitalized patients with serious infections. Specifically, this invention also discloses a pharmaceutical composition further including an excipient such as CVMC agent and is available in dry powder form for reconstitution before injection with a suitable solvent. The pharmaceutical compositions of this invention have been found normally to enhance resistance to precipitation in solutions to be administered parenterally. The invention also gives details of the dosage forms stored in sealed containers to be reconstituted before use. The invention further provides a process to manufacture these compositions and also a method of treating a subject having non-ocular infective conditions due to multi drug resistant bacterium.
WO2014029016A1 Compositions comprising a glycylcycline and a tyrosine kinase inhibitor for treating cancer Methods, kits and compositions for treating a cancer, the method comprising administering to a subject in need thereof a glycylcycline, for example tigecycline, and a TKI, wherein the glycylcycline and the TKI are provided in a synergistic ratio.
US20110130469 Compositions and methods relating to resveratrol The present invention relates to compositions and methods comprising resveratrol and uses thereof. Some embodiments include compositions and methods with increased bioavailability of resveratrol. Certain embodiments include compositions comprising resveratrol and a solubilizer. Particular embodiments include transmucosal delivery of resveratrol from the composition.
WO2014151529A1 Therapeutic agents and methods for the treatment of dna repair deficiency disorders The present invention provides compounds, compositions, kits, and methods which are effective for mitigating, treating, or ameliorating a DNA repair-deficiency disorder or a symptom of a DNA repair-deficiency disorder. The compounds, compositions, kits, and methods are also effective for modulating a level or activity of a DNA repair enzyme or a level or activity of gene encoding a DNA repair enzyme.
CA2464243C Method and composition for dry eye treatment A method and composition for treating a dry eye condition by topically applying to the eye surfaces an emulsion forming a tear film that acts to lubricate the eye and to inhibit evaporation therefrom. The emulsion is constituted by water in which is dispersed a mixture that includes a phospholipid, a non-polar oil, a non-toxic emulsifying agent and a polar lipid that imparts a net positive charge to the film that is distributed throughout the film, causing the film to be electrostatically attracted to the anionic surface of the eye whereby the film adheres thereto and cannot be washed away. Includable in the mixture is a non-soluble therapeutic agent, such as cyclosporin which is effective against an eye disease and is delivered to the eye by the film.
CN1850097A Scutellarin injection preparation and its preparing method The present invention relates to a breviscapine injection preparation and its preparation method. It includes a water injection preparation formed from breviscapine-Na and aqueous solution stable system composed of medicinal organic alkali whose pH value is 7-8 and organic acid. The medicinal excipient also can be added into the above-mentioned material for making water injection preparation so as to obtain the invented breviscapine freeze-dried powder injection preparation. Besides, said invention also provides the concrete steps of its preparation method.
CN102603694A Novel synthesis method of murrayone and novel application of murrayone The invention relates to the technical field of pharmaceuticals, in particular to a novel synthesis method of murrayone and novel application of murrayone in the preparation of drugs for preventing and treating osteoarthritis. The novel synthesis method of murrayone comprises the following steps: reacting 2,6-dimethoxyphenylacetic acid with boron tribromide to prepare 2-hydroxy-6-methoxyphenylacetic acid; reacting the 2-hydroxy-6-methoxyphenylacetic acid with ethyl propiolate to prepare 7-methoxy-8-acetoxy coumarin; reacting the prepared 7-methoxy-8-acetoxy coumarin with solid phosgene to prepare an acyl chloride compound at first, then adding dimethylamine to prepare 7-methoxy-8-(N,N-dimethyl acetamido) coumarin; and reacting the prepared 7-methoxy-8-(N,N-dimethyl acetamido) coumarin with a Grignard reagent such as isopropenyl magnesium bromide to prepare murrayone. Compared with the prior art, the required raw materials are easily accessible, the reaction conditions are mild, and the operation is simple.
CN101385696A Sodium alginate microspheres blood vessel suppository containing etoposide and preparation method and uses thereof The invention belongs to the field of medical embolization devices, relates to a sodium alginate microsphere targeted vascular embolization agent containing an antineoplastic drug and a preparation method thereof. Alginic acid is taken as a pharmaceutical carrier, the antineoplastic drug etoposide is a pharmaceutical active ingredient, divalent metal cation or calcium ion solution is taken as a solidifying agent, and the sodium alginate encapsulates the etoposide to prepare ideal particle size-controllable sodium alginate microspheres comprising the etoposide, thus avoiding toxic side effect of traditional etoposide administration such as anaphylaxis and inconvenience. The vascular embolization agent changes the dosage form and route of administration way of the antineoplastic drug etoposide, has high efficacy and low toxicity, and is safely and effectively applied to clinical application. The vascular embolization agent has the advantages of mild preparation condition and simple and convenient operation, and is fit for large-scale production. The vascular embolization agent can be used for vascular embolization, local targeted tumor treatment, and treating small-cell carcinoma of the lung, oophoroma, carcinoma of testis, gastric cancer and liver cancer by administering the vascular embolization agent during operations.
CN101564538A 3, 5-dihydroxy-4-isopropyl diphenyl ethylene-butanedioic anhydride-polyoxyethylene compound and synthetic method thereof The invention discloses a 3, 5-dihydroxy-4-isopropyl diphenyl ethylene-butanedioic anhydride-polyoxyethylene compound, namely polyoxyethylene-butane diacid-di(4-isopropyl-5-hydroxy diphenyl ethylene-3-phenolic ester). The original medicine is 3, 5-dihydroxy-4-isopropyl diphenyl ethylene (tolylene maud); and the modifier is polyoxyethylene and the linker arm is butanedioic anhydride. The synthetic method of the compound includes two esterification reactions. Compared with the original medicine, the compound has enhanced water-solubility and stability; the internal medicine distribution is changed; the bioavailability is enhanced; the synthetic method is simple; the reaction condition is mild; and the cost is low, without numerous unpleasant experimental procedures. In the method, the 3, 5-dihydroxy-4-isopropyl diphenyl ethylene-butanedioic anhydride-polyoxyethylene compound can be easily made.
CN103655528A Application of benzoquinone compounds in improving antioxidase expression to suppress pathology phenomena related to inflammations The invention relates to an application of benzoquinone compounds in improving antioxidase expression of mammals to suppress pathology phenomens related to inflammations, and a medical composition and a supplement which are prepared by the benzoquinone compounds. The benzoquinone compounds comprise a structure shown as a compound (I). In the compound (I), R1 represents a hydrogen group or [(C4H4)CH3]n; n is an integer ranging from 1 to 5; and R2 represents a hydrogen group or a methoxy group.
WO2011099886A1 Β-carbonyl derivatives having anti-tuberculosis activity The invention pertains to the field of medicine and pharmacology and relates to 1-(1- benzylindol-3-yl)2,3,4,9-tetrahydro-1-H-β-carbonyl derivatives of the general formula (I), which have an anti-tuberculosis activity; the invention also relates to the use thereof for preparing a therapeutic agent for treating tuberculosis, to a therapeutic agent containing the same for treating tuberculosis, to a method for synthetizing the same and to a method for treating tuberculosis.
CN102068436B Dihydroporphin photosensitizer and preparation and application thereof The invention discloses a dihydroporphin photosensitizer and preparation and application thereof. The name of the photosensitizer is meso-tetra (3-(4-morphlinomethyl)-4-methoxyphenyl) dihydroporphin, and the photosensitizer has the following chemical structural formula; and the preparation comprises the following steps of: reducing meso-tetra (3-(4-morphlinomethyl)-4-methoxyphenyl) porphin through a reducing agent, and performing column chromatography separation and purification. The photosensitizer has strong absorption in a visible light long wavelength area, and can be used for treatment of tumors of deep part and large volume; because the polarity of the compound is relatively low and the compound can be distributed on superficial pathological change tissues, the compound can also be used for treatment of superficial tumors; and the synthesis method for the compound is simple, and the compound can be conveniently prepared into hydrochloride, so the compound is easily prepared intoinjection for use and the stability of the compound can be enhanced. The photosensitizer can be applied in preparation of medicaments for treating tumor diseases or light-activated insecticides, and has broad application prospect.
EP2786782A1 Sulphated hyaluronic acid for treating degenerative osteoarthritis This invention relates to intra-articular formulations comprising sulphated hyaluronic acid which are effective in the treatment of degenerative osteoarthritis.
CN102145021A Anti-inflammatory effective component extract of antrodia cinnamomea sporocarp, preparation method and application thereof The invention discloses an anti-inflammatory effective component extract of antrodia cinnamomea sporocarp, a preparation method and application thereof. The preparation method comprises the following steps of: drying the antrodia cinnamomea sporocarp; and extracting the dried antrodia cinnamomea sporocarp by using ethanol, and collecting an ethanol extract to obtain the anti-inflammatory effective component extract of the antrodia cinnamomea sporocarp. In order to achieve the better extraction effect, the method comprises the following steps of: concentrating the ethanol extract further; layering a concentration product by using water and ethyl acetate; and collecting an ethyl acetate extract to obtain the anti-inflammatory effective component extract. The anti-inflammatory effective component extract of the antrodia cinnamomea sporocarp and Antrocamphin A separated from the antrodia cinnamomea sporocarp can reduce the expression of nitric oxide synthase or cycloxygenase 2 to inhibit pro-inflammation molecules from generating.
EP2051987A2 Use of cd83 in combination therapies The present invention relates to improved methods of suppressing and/or preventing an undesired immune response comprising the use of CD83. In some embodiments, CD83 is coadministered to a subject with at least one other immunosuppressive compound. Methods are also provided for generating tolerogenic dendritic cells and regulatory T cells. These cells can be used in vitro to produce additional cells for therapeutic purposes or they can be used in vivo to suppress and/or prevent an undesired immune response. Methods of the invention can be used to prevent or reduce the severity of autoimmune diseases and can also be used to induce tolerance to at least one therapeutic composition, such as a therapeutic protein or transplanted tissue.
EP1173197B2 Metabolic intervention with glp-1 to improve the function of ischemic and reperfused tissue Individuals in need of treatment of ischemia-related reperfusion are treated, preferably intravenously, with a composition which includes a compound which binds to a receptor for the glucagon-like peptide-1. The invention relates to both the method and compositions for such treatment.
US20100035910 Process for the Preparation of Quaternary N-Alkyl Morphinan Alkaloid Salts An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
WO2010069493A1 Improved combination of active agents comprising an antibiotic and a non-steroidal anti-inflammatory drug (nsaid) The invention relates to novel combination formulations in veterinary medicine, comprising a quinolone antibiotic and a non-steroidal anti-inflammatory drug (NSAID). The formulations, particularly injection solutions comprising a quinolone antibiotic and an anti-inflammatory substance, are particularly well suited for parenteral treatment of bacterial infections in animals such as cattle, swine, dogs, and cats.
CN1985812A Lung-targeting florfenicol microsphere for animal and birds and its preparing method The present invention belongs to the field of veterinary medicine technology, and is especially lung targeting florfenicol microsphere for animal and its preparation process. The florfenicol microsphere is prepared with florfenicol as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving florfenicol in gelatin solution and adding Span-80 and liquid paraffin through stirring to obtain emulsion; cooling in icy bath to below 5deg.c and adding glutaraldehyde through stirring for cross-linking and curing; dewatering with isopropyl alcohol and suction filtering; washing with isopropyl alcohol and ethyl ether to eliminate glutaraldehyd, washing with petroleum ether to eliminate liquid paraffin in the surface of microsphere and vacuum drying at room temperature to obtain florfenicol microsphere. The medicine has raised tissue selectivity, delayed release, raised curative effect and lowered toxic side effect.
CN102846663A Intravenous drip type body fluid replenisher The invention provides an intravenous drip type body fluid replenisher. The intravenous drip type body fluid replenisher is prepared by the following raw materials according to the following weight ratio: 500-900mg of sodium chloride, 20-40mg of potassium chloride, 50-100mg of calcium citrate, 50-100mg of calcium hydrogen phosphate, 5-20mg of zinc sulfate, 5-20g of copper sulfate, 10-20mg of ferrous sulfate, 50-150mg of water-soluble compound and 1000ml of purified water. The preparation steps are as follows: weighing various raw materials according to the weight ratio of a formula, adding water, dissolving and mixing the mixture uniformly, disinfecting at high temperature and high pressure, controlling the pressure to be 103.4kPa and the temperature to be 121.3 DEG C, maintaining for 15-20min, sampling to check the qualification, and then packaging to put in the storage.
CN1813732A External-use formulation of fexofenadine The present invention relates to a medicine fexofenadine preparation for external application. The pharmacological experiments show that said fexofenadine can obtain the obvious therapeutic effect for curing dermal allergic diseases.
CN101843584A Composite of all-trans-retinoic acid and liposome and application thereof The invention discloses a composite of all-trans-retinoic acid and liposome and application thereof. The composite of all-trans-retinoic acid and liposome consists of the liposome and the all-trans-retinoic acid encapsulated in the liposome. The composite is prepared by a method comprising: 1) dissolving lipid materials and the all-trans-retinoic acid to prepare a mixture of a lipid membrane and the all-trans-retinoic acid; 2) hydrating the mixture of the liquid membrane and the all-trans-retinoic acid to prepare a hydration product; and 3) performing ultrasonic on the hydration product to prepare the composite of the all-trans-retinoic acid and the liposome. Experiments of the invention prove that the composite of the all-trans-retinoic acid and the liposome can be used for inhibiting the reproduction of tumor cells, and the combined application of the composite of the all-trans-retinoic acid and the liposome and Vinorelbine invisibile liposome produces the strongest inhibitory effect on the recrudesce of tumors.
US20080039409 Method of Suppressing Cancer The present invention provides a method for suppressing cancer comprising activating tumor suppressor gene p53 or protein p53 for localizing the protein to the nuclear, and a pharmaceutical composition comprising a substance that promotes activation of tumor suppressor gene p53 or protein p53.
CN101282725A Diabetes-treating agent The present invention provides an agent for the prophylaxis or treatment of diabetes, which is associated with a ferwer side effects such as body weight gain, adipocyte accumulation, cardiac hypertrophy and the like, and which contains a compound represented by the formula (I), wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
US20110257142 Method for preparing 4-[17beta-methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11-beta-yl]benzaldehyde (e)-oxime (asoprisnil) The present invention relates to a method for the reliable and reproducible preparation of 4-[17β-methoxy-17α-methoxymethyl-3-oxoestra-4,9-dien-11β-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).
WO2006052189A1 Nitro indazole derivatives Compounds of Formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3 and R4 are as defined in the specificationas well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
WO2011160146A1 Pharmaceutical preparation containing dextran and sodium hyaluronate for the treatment of joint disorders Pharmaceutical preparation for intraarticular injection for treating inflammatory and degenerative joint disorders containing 0.2-32% (m/v) dextran with an average molecular weight of 500 to 3,000 Da and 0.1-10% sodium hyaluronate with an average molecular weight of 500,000 to 3500,000 Da, with the proviso that no further dextran having an average molecular weight in the range of 30,000 and 110,000 Da is contained.
WO2008069652A1 Combinations of a sphingolipid and an hmg-coa reductase inhibitor for treating hypercholesterolemia The present invention relates to the use of a sphingolipid and a cholesterol lowering agent, wherein said cholesterol lowering agent is a HMG-CoA reductase inhibitor, for the manufacture of a combined preparation for simultaneous, separate or sequential use in the treatment of hypercholesterolemia in a subject in need thereof.
US20100063009 Pharmaceutical Combination Comprising 6-Dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1.3-diol and an NSAID A combination comprising (a) at least one 6-dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol component, and (b) at least one non-steroidal anti-inflammatory drug (NSAID) component; a pharmaceutical composition and a dosage form comprising such as combination, and a method of treating pain and/or ostheoarthritis in a mammal characterized in that components (a) and (b) are administered simultaneously or sequentially to said mammal, in which component (a) may be administered before or after component (b), and in which components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.
WO2008038807A1 External composition for skin It is intended to provide an external composition for skin capable of imparting a physical feeling of stimulation to the skin, replacing pruritus such as particularly insect bites or hypersensitive skin with a feeling of stimulation, and effectively suppressing pruritus. The external composition for skin is characterized by containing butylhydroxytoluene in a solid state.
WO2010022055A3 1, 3, 5 -triaz ine derivatives useful in the treatment of chronic pain disorders The present invention provides compounds that are inhibitors of voltage-gated sodium channel (Nav), in particular Nav 1.7 and are therefore useful for the treatment of diseases 5 treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
WO2006048894A1 Novel crystalline forms of atorvastatin calcium and processes for preparing them. The invention describes novel Atorvastatin Polymorphs designated as M-2, M-3 and M-4 having substantially different XRD from those of the reported Forms and processes for the preparation thereof. The process comprises crystallizing the desired form using atorvastatin in solid or liquid form, ecologically friendly solvent such as aliphatic ketones exemplified by acetone, diethyl ketone, ethyl methyl ketone as solvent and antisolvent selected from water by varying ratio of the reactants, process parameters.
US7285548 Urea substituted benzothiazoles The present invention relates to compounds of formula I wherein R1 and R2 are described herein, and their pharmaceutically acceptable salts thereof for the treatment of diseases, related to the A2A receptor.
CN103351395A Esterified podophyllum derivative with antineoplastic activity and preparation method and application thereof The invention discloses an esterified podophyllum derivative with antineoplastic activity and a preparation method and application thereof. According to the invention, 2-pyrazine pyrazine, 5-methyl-2-pyrazine pyrazine, theophylline acetic acid, fluoroquinolone acid and 2-quinoline carboxylic acid are subjected to esterification reaction with 4'-demethylepipodophyllotoxin, so that the esterified podophyllum derivative with the antineoplastic activity, expressed by the formula (V), can be obtained. The esterified podophyllum derivative acts on cancer cells by means of multiple ways and multiple target points, and thus has better antineoplastic efficacy. As indicated by the in vitro cell activity inhibition test, the esterified podophyllum derivative disclosed by the invention has excellent antineoplastic activity and low toxic and side effects, and can be made into antineoplastic drugs for clinic antineoplastic treatment.
CN103130686A N,N'-asymmetric diayl substitution urea compound and preparation method and purpose thereof The invention relates to N,N'-asymmetric diayl substitution urea compound of a general formula (I). A and B independently represent aryl, one-substitution or multi-substitution aryl, miscellaneous aryl and one-substitution or multi-substitution miscellaneous aryl. R1 and R2 independently represent hydrogen or C1-C8 alkyl or C1-C8 alkoxy or aromatic alkoxy or acyl or non-aromatic heterocycle substitution group or halogen or nitryl or trifluoromethyl or cyan. The invention further relates to a preparation method of the compound, active component medicine composition of the compound and application of the compound in preparing medicine for restraining new delhi metallo beta-lactamase (NDM-1) drug-resistant bacteria.
US7208479 Peritoneal dialysis solution containing modified icodextrins The present invention provides a peritoneal dialysis solution that contains heat stable osmotic agents such as D-glucitols, gluconic acids and alkylglycosides produced the reduction, oxidation or glycosylation of icodextrins respectively. As a result, osmotic agents that are stable under autoclaving or heat sterilization conditions are provided which reduces the amount of bioincompatible materials in the sterilized peritoneal dialysis solutions. Methods of preparing the D-glucitols, gluconic acids and alkylglycosides are disclosed.
WO2010081266A1 A new use of tetrahydropalmatine A new use of tetrahydropalmatine, which is the use of tetrahydropalmatine of formula (I) or its pharmaceutically acceptable salts in preparing medicament for inhibiting tumor cells proliferation in eucaryon and in preparing medicament for preventing and/or treating tumor. The results of the test in nude mice show that tetrahydropalmatine may inhibit the tumor growth effectively and the volume of the tumor is markedly smaller than the negative control. So tetrahydropalmatine which has been widely used in ease pain has excellent anti- tumor activity and may be used in preparing medicament for treating cancer, especially lung cancer. This invention expands the pharmaceutical uses of tetrahydropalmatine.
WO2012136937A1 Zinc n-acetyl taurinate for the treatment of prostate cancer The present invention relates to Zn N-acetyl taurinate of formula: (I) [CH3-CO-NH-CH2-CH2-SO3]- 2 Zn2+ for the use thereof for treating prostate cancer.
US20110229571 Pharmaceutical Compositions Comprising a Selective I1 Imidazoline Receptor Agonist and an Angiotensin II Receptor Blocker Pharmaceutical compositions containing selective imidazoline receptor agonists combined with angiotensin II receptor blockers, particularly, pharmaceutical compositions containing Moxonidine and Eprosartan mesylate, as well as the use of such compositions for the treatment of hypertension, especially in hypertensive patients suffering from type II diabetes or susceptible to developing type II diabetes.
CN1793154A 3,5-di-0-(4-chlorobenzoyl)-2-deoxide-D-erythro-furan glucoside and preparation process thereof The invention discloses a 3, 5-2-0-(4-chlorobenzene chlorobenzene)-2-deoxidising- D-red-furanoside that contains alpha body and beta body. The method includes the following steps: dissolving chlorine indicant into tetrahydrofuran, quickly adding to alcoholic solutioin, whisking and reacting, after reacting, vacuuming and steaming solvent to gain mixture of alpha body and beta body, taking separation by column chromatography to gain separated alpha body and beta body. The invention is easy to operate and has high yield, and no harmful to the environment. It could be used to compound antivirus or anticancer drug, and could be used to control gene expression.
US7968553 Tetrahydro-4H-pyrido[1,2-a] pyrimidines useful as HIV integrase inhibitors Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
US20100303822 Polypeptides from non-typeable haemophilus influenzae Polypeptides comprising non-typeable Haemophilus influenzae (NTHi) amino acid sequences. Over 2500 specific NTHi proteins are disclosed. The invention also provides related polypeptides, nucleic acids, antibodies and methods. These can all be used in medicine for treating or preventing disease and/or infection caused by H. influenzae, such as otitis media.
CN103242321A Benzylpiperazine compound and anti-tumor application thereof The invention provides a preparation method of a benzylpiperazine compound and an anti-tumor application thereof. The benzylpiperazine compound is as show in a formula I. The benzylpiperazine compound of the formula I and salts thereof have an inhibition function on human lung cancer cells, human gastric carcinoma cells, human prostate cancer cells, myeloma cells and the like, and can be used for preparing pharmaceuticals for treating human lung cancer, human gastric cancer, human prostate cancer and myeloma.
CN102000030B Arbidol dry suspension and preparation method thereof The invention discloses an arbidol dry suspension and a preparation method thereof, and belongs to the medical industry. The arbidol dry suspension comprises Arbidol hydrochloride, a suspending aid, a diluent, a lubricating agent, a flavoring agent and a pH regulator, wherein the suspending aid is one or more of Arabic gum, tragacanth, sodium alga acid, povidone, hydroxy propyl cellulose and xanthan gum; the diluent is saccharose, mannitol and microcrystalline cellulose; the lubricating agent is lauryl sodium sulfate and sodium lauryl sulphate; the flavoring agent comprises a sweetener and anaromatizer, the sweetener is mannitol, saccharose, sodium cyclamate and aspartame, and the aromatizer is orange essence, banana essence, strawberry essence, and pineapple essence; and the pH regulator is citric acid and tartaric acid. The preparation method comprises the following steps of: sieving the arbidol hydrochloride, and respectively crushing and sieving the suspending aid, the diluent, and the lubricating agent; fully mixing the components except the diluent, and then adding the diluent for uniform mixing; and wetting by using ethanol to prepare a soft material, drying, and packaginginto an aluminum-plastic composite membrane bag. After the arbidol is prepared into the dry suspension, the bitter of the arbidol is effectively masked, and the compliance of the patient is greatly improved.
EP2060563A1 Cyclic aminoalkylcarboxamide derivative The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group and the like, R3 is a hydrogen atom, a C1-6 alkyl group and the like, R4 and R5 are the same or different and each is a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group and the like, X is a single bond or -C(R6)(R7)-, R6 and R7 are the same or different and each is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group and the like, or R6 and R7 optionally form, together with the carbon atom bonded thereto, an optionally substituted C3-8 cycloalkyl group and the like, ring group A is an azetidin-1-yl group and the like, m is 0, 1 or 2, and n is 0, 1 or 2.
US20070275083 ameliorating chronic renal insufficiency, hypertension, atherosclerosis, and chronic congestive heart failure The present invention provides for the identification, isolation and uses of mammalian Monoamine Oxidase C (MAO-C), also known as renalase.
CN103254126A Deuterated omega-diphenyl carbamide as well as derivative and pharmaceutical composition including compounds The invention relates to deuterated omega-diphenyl carbamide as well as a derivative and a pharmaceutically acceptable salt thereof. The invention further relates to a pharmaceutical composition including a pharmaceutically acceptable carrier, deuterated omega-diphenyl carbamide and the derivative and pharmaceutical and the pharmaceutically acceptable salt. The deuterated omega-diphenyl carbamide disclosed by the invention can be used for treating and preventing cancers and associated diseases.
CN103319467A 4-[5-hydroxy-pyrone-2-ylmethyleneanimo]-3-sulfydryl-1,2,4-triazole compound and application thereof The invention provides a novel 5-substituted-4-[5-hydroxy-pyrone-2-yl-methyleneanimo]-3-sulfydryl-1,2,4-triazole compound. The structural formula of the compound is as shown in a formula (I), wherein the substituent R is -CH3, -CF3, -CH2CH3, C6H5-, 3-CH3OC6H4, 4-CH3OC6H4-, 4-HOC6H4-, 2-CH3C6H4-, 3-CH3C6H4-, 4-CH3C6H4-, 4-C1C6H4-, 3-C1C6H4-, 4-BrC6H4-, 3-BrC6H4- or 3,5bitertiary butyl-4-hydroxy phenyl. The 5-substituted-4-[5-hydroxy-pyrone-2-yl-methyleneanimo]-3-sulfydryl-1,2,4-triazole compound provided by the invention has certain inhibitory activity for tyrosinase, and can be used for preparing skin whitening cosmetics and medicines. In addition, the synthesis method is simple, and materials are available.
WO2007011721A1 Inhibitors of mitotic kinesin The present invention relates to compounds useful as inhibitors of KSP and methods for the treatment or prevention of cellular proliferative diseases.
US20080175892 fullerene carbon nanotube linking to paclitaxel through polyethylene glycol, serinol, succinimidyl-3-(2-pyridyldithio)-propionate or succinic acid; anticarcinogenic agents treating lung cancer; drug target with antibody; aerosols drug delivery Nanostructure-drug conjugates and associated methods of use are provided. In one embodiment, a nanostructure-drug conjugate comprising a Cn, a crosslinker, and a drug is provided, wherein Cn refers to a fullerene moiety or nanotube comprising n carbon atoms. A method of treating cancer is also provided, comprising administering a therapeutically effective amount of a nanostructure-drug conjugate comprising: a Cn, a crosslinker, and a drug, wherein Cn refers to a fullerene moiety comprising n carbon atoms to a mammal.
CN102698249A Injection for treating encephalatrophy The invention relates to the technical field of medicine, in particular to an injection for treating encephalatrophy. The injection provided by the invention comprises a certain amount of ginkgodipyidamolum, cerebroprotein hydrolysate, 22g of glutathione, Vit B6 and Vit B12, and is injected into a human body, wherein the cerebroprotein hydrolysate can be used for nourishing brain cells; the ginkgodipyidamolum can be used for dredging brain micro circulation; glutathione can be used for removing free radicals and repairing cell membranes; and vitamins can be used for nourishing brain cells. The injection has the characteristics of nourishing brain cells, repairing brain cell intima and dredging brain fine blood vessels, has the effect of recovering brain activity, improving brain cell function and improving memory, and can be used for completely improving encephalatrophy symptoms such as the hypomnesis, inattention, dull expression, slowness in movement, inconsonant actions, dithered limbs and the like.
US20130096166 Camalexin as a treatment for prostate cancer Compositions and methods to treat prostate cancer with the compound camalexin and its structural analogs. Camalexin increases ROS production and decreases the proliferation of prostate cancer cells, especially aggressive prostate cancer cells.
US20110293724 Enzyme Treatment of Foodstuffs for Celiac Sprue Administering an effective dose of glutenase to a Celiac or dermatitis herpetiformis patient reduces levels of toxic gluten oligopeptides, thereby attenuating or eliminating the damaging effects of gluten.
WO2010123111A1 1-menthyl (3r)-3-hydroxybutanoate, process for producing same, and composition containing same for stimulating sense An ingredient for imparting a cooling sensation or stimulating a sense, the ingredient imparting a more intense cooling sensation and having excellent retentivity of refresh feeling and cool feeling; a composition for stimulating a sense, which contains the ingredient; and various products each containing the composition for stimulating a sense. The ingredient for imparting a cooling sensation or stimulating a sense is 1-menthyl (3R)-3-hydroxybutanoate, which is represented by formula (I).
EP2167509A1 Piperazine and ý1,4¨diazepan derivatives as nk antagonists The present invention relates to a compound of Formula (I) wherein R1 is hydrogen or lower alkyl; is hydrogen, fluoro, hydroxy or lower alkyl; R3 is hydrogen or lower alkyl; R4 is -CHR5-A R5 is hydrogen, lower alkyl, fluoro, CF3, CH2OH or cycloalkyl; A is aryl or heteroaryl, which rings are unsubstituted or substituted by (R6)o; R6 may be the same or not when o is more than one, and is heteroaryl, lower alkyl, lower alkoxy, cyano, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or NR7R8; o is 1, 2 or 3; R7, R8 are independently hydrogen or lower alkyl; R9 is lower alkyl; R10 is lower alkyl, lower alkoxy or halogen; n is 1 or 2; m is 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. The invention includes all sterioisomeric forms, including individual diastereoisomers and enantiomers of the compound of Formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
CN101301472A Anticancer composition containing taxane medicament and bortezomib The invention provides a sustained-release injection which is an anti-tumor composite containing taxanes drug and bortezomib. The sustained-release injection comprises a sustained-release microsphere and a solution medium, wherein the sustained-release microsphere comprises effective anti-tumor ingredient and sustained-release excipient, the solution medium is a common solution medium or a special solution medium containing a suspending drug. The suspending drug has the viscosity between 100cp and 3000cp (under twenty centi degrees to thirty centi degrees) and is selected from sodium carboxymethylcellulose and others; the effective anti-tumor ingredient comprises the anti-metabolite drug and/or the combination thereof; the taxanes drug is selected from Taxol, Docetaxel, EPI-Taxol or Hydroxy-Taxol; the sustained-release excipient is selected from polyphosphonate copolymer like p(LAEG-EOP)or p(DAPG-EOP), PLA, PLGA, polyphosphonate with PLA, polifeprosan and the polymer or blending polymer of ( erucic acid dipolymer-sebacic acid) or poly(boletic acid-sebacic acid); the anti-tumor composite can also be prepared to be a sustained-release implant which can maintain the effective concentration of drug over forty days for intratumor or tumor circumference injection or placement, can also reduce general reaction obviously and enhance the treatment effect of non-operative therapeutics such as chemotherapy and radiotherapy.
EP1713477B1 Combination of voriconazole and an antifungal cyp2c19 inhibitor The invention provides a therapeutic combination comprising voriconazole and an antifungal CYP2C19 inhibitor in specific quantities and weight ratios. Pharmaceutical compositions, unit dosage forms and kits comprising voriconazole and an antifungal CYP2C19 inhibitor, and their use in the treatment of fungal infections, are also provided.
US20090192194 Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them A compound of formula (I) wherein R is a radical selected from in which R7 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; p is an integer from 0 to 3; R1 is hydrogen, halogen, cyano, C2-4 alkenyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy; R2 is hydrogen or C1-4 alkyl; R3 and R4 independently are hydrogen, C1-4 alkyl or R3 together with R4 is C3-7 cycloalkyl; R5 is phenyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, naphthyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, a 9 to 10 membered fused bicyclic heterocyclic group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl or R5 is a 5 or 6 membered heteroaryl group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl; R6 is hydrogen or (CH2)qR8; R8 is hydrogen, C3-7 cycloalkyl, C1-4 alkoxy, amine, C1-4 alkylamine, (C1-4 alkyl)2amine, OC(O)NR9R10 or C(O)NR9R10; R9 and R10 independently are hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m is zero or 1; n is 1 or 2; q is an integer from 1 to 4; r is 1 or 2; or pharmaceutically acceptable salts and solvates thereof; processes for their preparation to pharmaceutical compositions containing them and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.
CN1631365A Sodium salinomycin powder and its preparation Disclosed is a sodium salinomycin powder and its preparation, which comprises the steps of fermentation liquor acidification and deactivation, sedimentation and concentrating, adjusting pH, charging adjuvant and medicinal bonding agent, charging bottom flavoring into fluid bed hopper, spray drying, spraying dried particles, mixing and sieving. The bonding agent can be alpha-starch, carboxymethy Icellulose sodium and carboxymethyl cellulose sodium.
US7189720 Selective NPY (Y5) antagonists This invention is directed to triazine derivatives, bicyclic compounds and tricyclic compounds which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. This invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.
CA2263584C Orally applicable formulation of quinolone or naphthyridone carboxylic acids Orally applicable formulations of quinolone or naphthyridone carboxylic acids are prepared by mixing quinolone or naphthyridone carboxylic acids as such or in the form of their water-soluble salts or derivatives, preferably in the form of their aqueous salt solutions, with embonic acid as such or in the form of its water-soluble salts or derivatives, preferably in the form of its aqueous salt solution, in the presence of an excipient, optionally in the presence of auxiliary substances, in the case of dry mixtures in the presence of water, and if required by giving to the thus obtained mixture other forms ready for use.
US20100016207 Methods and Compositions for Raising Levels and Release of Gamma Aminobutyric Acid The present invention provides methods of increasing the level or release of gamma aminobutyric acid (GABA) in the brain, treating Alzheimer's disease, Huntington's disease, symptoms thereof, anxiety, aggression, insomnia, cognitive or memory disturbances; seizures of any cause (e.g. idiopathic epilepsy), primary or metastatic brain tumors, depression (e.g. bipolar depression), or pain (e.g. neuropathic pain), comprising administration of glutamine, a salt thereof, or a glutamine-rich peptide. The present invention also provides methods for decreasing the level or release of GABA in the brain and treating hepatic encephalopathy, depressed consciousness, and coma, comprising decreasing dietary intake of glutamine.
US20100291025 Indazole inhibitors of tyrosine kinase The present invention relates to new indazole inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.
CN101904838A Application of ligustilide in preparing composition for preventing and treating senile dementia The invention relates to an application of ligustilide in preparing a composition for preventing and treating senile dementia, which comprises ligustilide as an effective component and other components acceptable pharmaceutically and/or acceptable in food or auxiliary components. As required, the effective components can comprise at least one of acetylcholinesterase inhibitor, excitatory amino acid and peptide transmitter components, Abeta fibration and sedimentation disturbance components, antioxidant, microcirculation improving components and calcium antagonist accounting for 10%-40% of the total weight. Shown by experimental results, through the protective actions of the ligustilide on damage caused by oxidation, apoptosis and inflammatory reaction induced by the Abeta amyloid peptide fragment and aging neuron degenerative change, the composition can obviously improve the descending of learning and memory caused by the Abeta amyloid peptide fragment and the aging neuron degenerative change, and can be used as a medicine and/or a health food composition.
CN103203008A Pharmaceutical composition for sobering up and preparation method thereof The invention discloses a pharmaceutical composition for sobering up and a preparation method thereof. The pharmaceutical composition comprises the following components in parts by weight: 55-65 parts of orange peel, 25-35 parts of tea leaf, 65-75 parts of kudzuvine root, 55-65 parts of raisin tree seed, 75-85 parts of lalang grass rhizome, 65-75 parts of common lophatherum herb, 45-55 parts of liquorice root, 95-105 parts of raw olive fruit, 95-105 parts of raw Chinese wampee fruit, 0.6-1.0 part of L-cysteine and 4.0-5.0 parts of corn peptide. The pharmaceutical composition disclosed by the invention is finely mixed by an inventor by adopting pure natural medicines or components extracted from natural plants. The pharmaceutical composition disclosed by the invention has the effect of protecting the liver, and can thoroughly relieve nausea, vomiting, headache and other symptoms after a person is drunk.
US20070191320 Methods of treatment for female sexual arousal disorder The invention provides methods of treatment for female sexual arousal disorder. In preferred embodiments, the invention provides methods of treatment with a semisolid composition suitable for topical application comprising: an effective amount of a vasoactive prostaglandin, a penetration enhancer, a polymer thickener, a lipophilic component, water and an acidic buffer system.
US20100311688 Ophthalmic formulations, methods of manufacture, and methods of using same The present invention provides compositions for treating and/or preventing signs and symptoms associated with dry eye and/or ocular irritation, and methods of use thereof. Such compositions are provided in novel ophthalmic formulations that are comfortable upon instillation in the eye. Methods of manufacture are also provided.
WO2011032192A1 Substituted clavulanic acid The present invention relates to compounds of the formula (I) and to an intermediate of the formula (II), wherein the substituents have various meanings. Said compounds can be used as ß-lactamase inhibitors.
US20120148678 Sustained release of poorly water soluble active compounds We have disclosed an implantable sustained release composition comprising, a biocompatible, biodegradable polymer, a cyclodextrin inclusion complex of a poorly water soluble pharmaceutical agent present, and a plasticizer, where the polymer is the minority phase of the formulation. Furthermore, The we disclose an implantable sustained release composition that provides a detectable plasma level of an otherwise poorly soluble drug for at least 28 days.
EP2280714A1 Compositions comprising anrnox-inhibitors for the inhibition of reactive oxygen species The invention relates to agents for sequestering serum aging factors, and methods for using the same. More particularly, the invention relates to agents termed herein 'Naractin' to denote any one of several naturally-occurring arNOX inhibitors either present in N. tazetta powder or capable of augmenting N. tazetta powder to an inhibitory level comparable to that of the fresh N. tazetta extracts, and to methods for using 'Naractins' to prevent or treat disorders and complications of disorders resulting from cell damage caused by an aging-related isoform of NADH oxidase (arNOX). In one exemplary embodiment the agents of the invention comprise at least one naturally occurring Naractin. Such naturally occurring naratins are also capable of augmenting the anti-arNOX effect of other naturally occurring arNOX inhibitory agents.
WO2007131365A1 Treatment of neoplastic disorders using a farnesyl dibenzodiazepinone administered by continuous intravenous infusion This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms by administration of the farnesylated dibenzodiazepinone compound of Formula (I) via continuous intravenous infusion. The invention includes pharmaceutical compositions comprising the compound of Formula (I).
US7001910 substituted pyrimidinyl-amino-ethoxy benzyl-thiazolidine-diones; hypoglycemic agents The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for their production and to their use as antidiabetic and *hypoglycemic agents, alone or in combination with other antidiabetic agents, such as sulfonilureas or biguanides, as well as for the treatment of complications associated to the resistance to the insulin, such as hypertension, hyperuricemia or other cardiovascular, metabolic, endocrine conditions, or other conditions related with diabetes.
CN102210809B Lotion for treating onychomycosis The invention relates to a lotion for treating onychomycosis, prepared from the following raw materials in parts by weight: 4-8 parts of Chinaberry seed, 8-10 parts of madder, 6-10 parts of sulfur, 10-14 parts of phellodendron bark, 6-10 parts of argyi leaf, 6-10 parts of thistle, 5-10 parts of Chinese atractylodes, 6-8 parts of woolyfruit stylophorum herb, 8-10 parts of bracken, 6-8 parts of panicled swallowwort root, 12-16 parts of sealwort, 10-12 parts of dittany bark and 8-14 parts of chuanxiong rhizome. The lotion for treating onychomycosis has the beneficial effects of good curative effect, short course of treatment, small side effect, convenience in use and low cost, and the product has good effects on sterilizing fungi causing the onychomycosis, is safe and reliable in use, and isconvenient and sanitary.
WO2012086406A1 Glp-1 secretagogue Provided is a substance useful for such purposes as promoting GLP-1 secretion, suppressing glucagon secretion, suppressing appetite, or preventing and/or mitigating post-prandial hyperglycemia, and illnesses or conditions such as diabetes. A lysophosphatidylinositol or salt thereof is used to promote GLP-1 secretion. A lysophosphatidylinositol or salt thereof is used to produce a GLP-1 secretagogue. A method for promoting GLP-1 secretion comprises either administering or feeding a lysophosphatidylinositol or salt thereof to a subject.
US20110172261 DIBENZO[f,h]ISOQUINOLINE DERIVATIVES A group of novel dibenzo[f,h]isoquinoline derivatives as shown in the specification. Also disclosed are methods of using the compounds for treating a disease associated with NO overproduction, cancer, or viral infection.
CN103446113A Applications of Sarcaboside B in medicament for treating dengue virus infection The invention discloses applications of Sarcaboside B in preparing a medicament for treating dengue virus infection. The Sarcaboside B can effectively inhibit the proliferation of dengue virus, and can be further developed into a medicament for treating dengue virus infection-caused diseases due to low cell toxicity, thus having wide application prospects. The applications of the Sarcaboside B in preparing the medicament for treating or preventing the dengue virus infection are disclosed for the first time. As a skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpectedly strong dengue virus inhibition activity, and the possibility of giving any inspiration by other compounds does not exist. The Sarcaboside B has significantly substantive characteristics, as well as obviously prominent progress in the prevention and treatment of the dengue virus infection.
CN101735329A Pholiota adiosapose polysaccharide and preparation method thereof The invention provides pholiota adiosapose polysaccharide, which is extracted from a pholiota adiosapose mycelium or fruiting body and prepared by purification, is a heteropolysaccharide comprising four monosaccharides, namely glucose, fructose, mannose and galactose, can improve body immunity and has functions of preventing cancers, resisting cancers, resisting ageing and the like, and can be used in combination with ganoderma lucidum polysaccharide, coriolus versicolor polysaccharide and the like. The invention also provides a method for preparing the pholiota adiosapose polysaccharide. The method is an improvement on water extract method and makes the yield of the polysaccharide reach over 23 percent, the content of the polysaccharide reach 55 percent, and the growth amount of the mycelium after the crude polysaccharide is purified up to 93.67 percent. Combined with a mycelium liquid culture technique, the method can increase the growth amount of the mycelium by over 10 percent so as to decrease the production cost, improve the production efficiency and in particular greatly improve bioactivity of polysaccharide products.
CN103479614A Application of Spirooliganones B in preparation of medicines treating Alzheimer's disease The invention discloses a new use of Spirooliganones B, which has acetylcholinesterase inhibitory activity and a nerve cell protection effect. As a compound with multiple action targets, Spirooliganones B can be used for preparing drugs resisting Alzheimer's disease, and the use is disclosed for the first time. With a skeleton type belonging to a brand new skeleton type, the Spirooliganones B has strong inhibitory activity on acetylcholinesterase, and has outstanding substantive features. Meanwhile, the use of the Spirooliganones B in prevention and treatment of Alzheimer's disease obviously has significant progress.
US20090274720 Anti-dementia substance from hericium erinaceum and method of extraction A fat-soluble fraction extracted from the fruiting body of Hericium erinaceum is demonstrated to inhibit the neuronal toxicity of amyloid beta-peptide (Aβ) and induce the synthesis of nerve growth factor (NGF), and has great potential as an active ingredient for pharmaceutical products, health food products, food products and/or beverages to prevent and/or treat dementia, especially Alzheimer-type dementia. This invention is to provide the bioactive fraction and its preparation method.
EP1161418B1 1-acyl-7-nitroindoline derivatives, their preparation and their use as photocleavable precursors Photoreleasable compounds comprising a caging moiety linked to an effector moiety represented by structural formula (I) wherein R1 is hydrogen; C1-10 alkyl or substituted alkyl; O(CH2)n-Y; N(COZ)(CH2)mY; or N[(CH2)mY'[(CH2)NY]; R2 and R3 are independently selected from: hydrogen; C1-10 alkyl or substituted alkyl; or R2 and R3 together are cycloalkyl; R4 is hydrogen; C1-10 alkyl or substituted alkyl; phenyl or substituted phenyl; (CH2)nY; or (CH2)mO(CH2)nY; wherein m and n are independently between 1 and 10; Y and Y' are independently selected from hydrogen, CO2H or salts thereof or OPO3<2->; Z is hydrogen or C1-10 alkyl or substituted alkyl; and, X is an effector moiety or a group capable of being coupled or converted to an effector moiety, which are capable of releasing the effector moiety on irradiation, typically by flash irradiation with UV light. The photoreleasable compounds can therefore be used to deliver biologically active effector moieties such as neuroactive amino acids or metal chelators to sites where their activity is required.
US20070265227 Inhibition of hiv infection fhrough chemoprophyalxis A process is provided for protecting a primate host from a self-replicating infection by an immunodeficiency retrovirus. Protection is achieved by administering to the primate host a combination of a pharmaceutically effective amount of a nucleoside reverse transcriptase inhibitor and a pharmaceutically effective amount of a nucleotide reverse transcriptase inhibitor prior to exposure to the immunodeficiency retrovirus. The administration is effective if provided in a single dose within 24 hours of the exposure. A regime of regular daily doses is also effective in providing protection against an immunodeficiency retrovirus becoming self-replicating after infecting a primate host A process for controlling retrovirus transmission within a population includes the administration to a subpopulation at high risk for contracting an immunodeficiency retroviral infection the detailed combination prior to sexual exposure to a source of immunodeficiency retrovirus so as to preclude the immunodeficiency retrovirus from becoming self-replicating in a member of the subpopulation.
US20080161369 Open label, single arm, two stage, multicenter study; patients who have not responded to taxane/platinum therapy or have relapsed within six months The present invention relates to a method of treating a warm-blooded animal, especially a human, having a cancer disease selected from hepatoma; primary fallopian tube cancer; primary peritoneal cancer; breast cancer progressing after treatment with hormonal agents or radiotherapy; renal cell carcinoma progressing after treatment with a cytokine, radiotherapy and/or nephrectomy; melanoma progressing after radiotherapy; prostate cancer progressing after orchiectomy; ovarian cancer progressing after treatment with a platinum compound or radiotherapy; and colorectal cancer progressing after radiotherapy and/or treatment with oxaliplatin or irinotecan;and metastasis thereof comprising administering to said animal a therapeutically effective amount of an epothilone derivative of formula I
CN102531996A Disubstituted indolone derivative and preparation method and application thereof The invention belongs to the field of preparation methods of novel compounds, and particularly discloses a disubstituted indolone derivative and a preparation method and application thereof. A structural formula is as follow, wherein R1 is halogen, R2 and R3 are hydrogen, and R4 is carboxylic acid and methyl ester. In the application, the disubstituted indolone derivative is synthesized for the first time; the derivative possibly has quite good bioactivity; the process of a synthetic route is simple; and the yield of a product is high.
WO2013117299A1 Deuterated thiazolidinone analogues as agonists for follicle stimulating hormone receptor The present invention relates to deuterated thiazolidinone analogues as agonists for follicle stimulating hormone receptor and their use for treating fertility disorders.
CN103735497A Liquiritigenin injection and preparation method and application thereof The invention discloses a liquiritigenin injection and a preparation method and application thereof. Each 100mL of liquiritigenin injection provided by the invention contains 10mg-1000mg of liquiritigenin, 20-50mL of propylene glycol and the balance of injection water; the liquiritigenin injection has a pH value of 4.0-6.0. According to the liquiritigenin injection, through a plenty of experiments, the dissolving solvent and the consumption thereof of the liquiritigenin injection, the concentration of liquiritigenin, and the pH value of the injection are screened, and thus an optimal injection formula is obtained; meanwhile, according to the solubility, the stability, the vascular stimulation, the hemolysis and the like, a preparation process of the liquiritigenin injection is screened. Experiments indicate that the liquiritigenin injection prepared by adopting the preparation method is small in irritation, free from hemolytic activity, high in safety, especially better in stability, strong in anti-tumor activity, capable of overcoming the defects of serious first-pass effect, low bioavailability and the like of an existing preparation, and better in clinical effect.
US7351813 Expression vector coding heterologous protein for use in human therapeutics; for treatment of blood nd liver disorders In one aspect, the present invention provides nucleic acid expression cassettes that are predominantly expressed in the mammalian liver. The present invention also provides vectors comprising a nucleic acid expression cassette that is predominantly expressed in the mammalian liver. The present invention also provides methods of ameliorating the symptoms of a disease, the methods including the steps of introducing into the liver of a mammalian subject a vector comprising a nucleic acid expression cassette that encodes a polypeptide, and expressing a therapeutic amount of the polypeptide in the liver.
CN103285166A External-use tea medicine composition for treating dermatophytosis and preparation method thereof The invention discloses an external-use tea medicine composition for treating dermatophytosis. The medicine composition is prepared by the following components by weight part: 10-60 parts of aged Pu'er tea, 10-40 parts of aged Tie Guan Yin tea and 10-30 parts of aged black tea. The invention further discloses a method for preparing the external-use tea medicine composition. The medicine composition has reasonable formula, and aged Pu'er tea, aged Tie Guan Yin tea and aged black tea are used as the main materials and white vinegar is used as the medicinal guide when the medicine composition is used; the medicine composition is used for treating dermatophytosis from the internal causes and manifestations, the efficacy is accurate, and the recurrence rate is low; the medicine composition uses tea as the main materials, and has no any side effect when administrated for long time.
EP2442785A1 Agent for preventing or treating abnormality in skin water permeation function An object of the present invention is to provide a skin water permeation function enhancer that can adjust TEWL according to the skin condition to thereby normalize skin water permeation function, thus enhancing skin water content regulation effect. Purine nucleic acid have an action of properly adjusting TEWL according to the skin condition, and are therefore used as an active ingredient of a skin water permeation function enhancer.
US20090118296 Heteroaromatic Compounds As Inhibitors Of Stearoyl-Coenzyme A Delta-9 Desaturase Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease.
US20080269150 Intra-vascular kidney gene therapy with plasmid encoding BMP-7 The present invention relates to recombinant vectors expressing the BMP-7 polypeptide in host cells and to pharmaceutical compositions comprising such recombinant vectors. The invention also encompasses methods for prevention and/or treatment of both acute and chronic renal failure in mammals, advantageously in humans, dogs and cats, by intra-vascular kidney administration of the recombinant vectors and pharmaceutical compositions of the invention.
US20090227523 Use of compatible solutes as substances having free radical scavenging properties Methods of using compatible solutes cyclic 2,3-diphosphoglycerate (cDPG), 1,-di-glyccrol phosphate (DGP), firoin and firoin-A, and/or derivatives of these compounds or combinations thereof, for treating skin conditions such as dermatoses and age spots. The methods include the application to the skin of a cosmetic and/or dermatological preparation containing the compatible solutes.
EP1911451A1 Protein-kinase CK2 inhibitors and their therapeutic applications The present invention is related to novel protein-kinase CK2 inhibitors, their method of preparation and their use as anti-cancer, anti-viral or antiinflammatory drugs wherein Ar1, Ar2, Z1, Z2, Z3, Z4 and R5 are as defined in claim 1.
WO2010129337A3 New oral formulations for tetrapyrrole derivatives Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract.
US20050084505 Utilization of ubiquinones for influencing the effect of histamine Use of ubiquinones for reducing histamine activity.
CN101264318A Virosis vaccine oral liquid for livestock, poultry and marine lives animal and preparation thereof The invention relates to a composition and the preparation method for livestock, poultry and aquatic animals. The virus disease vaccine oral liquid comprises the following materials according to the weight account: loosestrife 12 to 25 parts, humifuse euphorbia 15 to 25 parts, tuber of dwarf lilyturf 10 to 20 parts, phyllanfhus 5 to 20 parts, bitter almond 10 to 25 parts, prunella vulgaris 15 to 25 parts, balloonflower 10 to 20 parts, snake gall 2 to 5 parts, ox gall 10 to 20 parts, aloe 40 to 60 parts, crystal sugar 25 to 40 parts, rimantadine 5 to 10 parts, ribavirin 10 to 15 parts, and colistin 10 to 20 parts. The composition has the advantages of ability to reinforce antibody immunity, to relieve mutual interference among vaccines, and to reinforce the immune effect of the vaccine, and convenient drinking water and administration, high absorptivity, wide distribution, no drug residue or poison or side effect, and wide safety range.
CN102000053A Application of paclitaxel and derivants thereof in pharmacy field The invention relates to novel application of paclitaxel and derivants thereof in the pharmacy field, in particular to application in the preparation of analgesics. When in use with low dose, a prepared product is safe and has no toxic and adverse effects, and has strong pharmacological action and good curative effect on analgesia.
CA2768095A1 Heterocyclic compounds as autotaxin inhibitors ii Compounds of the formula (I), where R1, R2, X, X1, Y, Y1, Q, E, n1 and n2 have the meanings indicated in claim 1, are autotaxin inhibitors and can be used for the treatment of tumors.
US6989398 Benzanilides as potassium channel openers Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.
CN101259161B Production technology of cream for treating toothache and odontitis The invention provides the manufacturing technique of cream that can treat toothache and odontitis. Glycerin, sodium carboxymethyl cellulose and sodium lauryl sulfate are evenly stirred and mixed in an oil phase boiler; purified water, borax and saccharine sodium are melted by heating in a water phase boiler; the colloid is prepared by evenly emulsifying the two phases which are sucked into the emulsifying boiler; and the colloid and calcium carbonate are evenly stirred in the emulsifying boiler and then prefumery compound, eugenol type basil oil and glycyrrhetinic acid ethanol solution are added into the emulsifying boiler to be evenly stirred, thus forming the cream. The manufacturing technique of the invention is simple and the manufactured cream has a good effect on treating the toothache and the odontitis.
CN101683492A Patch for treating facioplegia and method for producing the same The invention provides a patch for treating facioplegia and a method for producing the same. The invention contains the following components in proportion by weight: curcuma rhizome 5-10, rhizoma atractylodis 3-10, dried alum 3-10; the invention includes the steps of: proportionally mixing raw materials, grinding until particle diameter of each component is 100-200 mu m; using CO2 supercritical extraction, fractionating acquired distillates with a fractionating tower, mixing each component in the formula into nano medicinal pulp according to the formula proportionality through the nano dispersing apparatus, adding accelerating agent for percutaneous absorption and contact adhesive into the circular type low temperation drying coater, and after coating, executing shearing, quality test, packaging and then sending the product into warehouse. The invention uses a scientific method for processing and extracting medicinal materials, which are filled in the framework of the substrate, and the paster substrate has a good compatibility with skin, and is good for medicament molecule to pass; the medicament has the advantages of slow release, smooth and steady administration, small irritation, without toxic and side effects.
EP2376475A1 4-azetidinyl-1-heteroaryl-cyclohexanol antagonists of ccr2 The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).
WO2012173174A1 Azaspiroalkane compound Provided is a compound represented by general formula (I) and having an excellent GPR119 agonistic activity, or a pharmaceutically acceptable salt thereof. [In general formula (I), m1 represents an integer of 0-2; m2 represents an integer of 1-2; the ring represented by A represents a benzene ring or a 6-membered heteroaromatic ring; X represents -O- or -NR3-; and Y represents a C1-6 alkanediyl.]
WO2011111738A1 Novel fki-4429 substance and method for producing same Disclosed are substance FKI-4429-1 represented by formula [I] and three other substances. Filamentous bacteria having the capability of producing this substance FKI-4429-1 are cultured in a medium. The substance FKI-4429-1 accumulates in this culture. The substance FKI-4429-1 is collected from this culture. The other three substances are substance FKI-4429-2, substance FKI-4429-3 and substance FKI-4429-4. An antibacterial drug contains substance FKI-4429-1 and an aminoglycoside antibiotic.
CN102335138A Preparation method of nano-composite vitamin with anti-stimulation action and livestock universality The invention relates to a preparation method of nano-composite vitamin with anti-stimulation action and livestock universality. The method comprises the following steps: 1, dissolving vitamin A and vitamin E into peanut oil in which an anti-oxidant is added in advance, and adding a proper amount of surfactant and distilled water in which the anti-oxidant and a metal ion complexing agent are added to obtain a uniform and transparent solution; 2, dissolving sodium benzoate in the distilled water, gradually adding vitamin B1, vitamin B2, sodium phosphate, vitamin B6 and vitamin C, stirring for dissolving, gradually adding folic acid, nicotinamide and calcium pantothenate, respectively adding glycine, methionine, lysine, glutamic acid and threonine, uniformly stirring, finally adding glucose, mannanoligosaccharides and astragalus polysaccharides, and dissolving to obtain a transparent uniform solution; and 3, slowly adding the solution prepared in the step 2 into a solution system prepared in the step 1, uniformly stirring, and fixing volume by use of the distilled water in which the anti-oxidant and the metal ion complexing agent are added to obtain a transparent and stable nano-composite system.
EP1453743B1 Pharmaceutical product and method with an adsorbent Use of an adsorbent in preventing the formation of an adduct in a pharmaceutical product due to a chemical reaction between a medicament and a gaseous substances released by a component of a medical device packaged with the medicament.
WO2006132217A1 Crystal of salt of benzimidazole compound A crystal of a salt of 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole which is useful as a medicine, and use of the crystal.
EP1274450B1 Medical uses of agonsist and antagonists of IL-174 Agonists or antagonists of cytokine designated IL-174, and various methods of their use are provided. In particular, the methods make use of facts that many activities of the IL-174 cytokine are described.
WO2014069655A1 Immune-tolerance inducer The purpose of the present invention is to create an immune-tolerance inducer used in therapy in which donor hematopoietic cells are transplanted into a recipient in order to induce immune tolerance in the recipient with respect to donor cells, tissue, or organs. By using an alpha-galactosylceramide-containing liposome in combination with a costimulatory-pathway-blocking substance, hematopoietic chimerism can be induced in the recipient by the transplantation of donor hematopoietic cells, making it possible to induce immune tolerance in the recipient with respect to donor cells, tissue, or organs.
CN102038190A Application of ampelopsin to preparation of anti-mutagenic health-care foods and medicaments The invention discloses application of ampelopsin to preparation of anti-mutagenic health-care foods and medicaments. Pharmaceutically allowable oral formulations, injection formulations or externally applied formulations are prepared from purified ampelopsin or unpurified ampelopsin-containing extracts.
CN101171927A Choline-silicic acid complex with osmolytes and divalent trace elements The present invention relates to a biological preparation comprising orthosilicic and silicic acid, a primary (''constant/first'') osmolyt choline and a weak alkalinizing agent without free hydroxyl groups and to a method for preparing the preparation, comprising: i) hydrolysing a silicon comprising choline solution thereby forming a choline stabilized orthosilicic acid and oligomers solution; ii) alkalizing the choline orthosilicic acid and oligomers solution by adding a weak alkalizing agent without hydroxyl groups; and iii) optionally adding a divalent trace element and/or secondary osmolyte, to biological preparation obtainable and its uses.
EP1037622B1 Taurine derivatives usable in the treatment of retinal disorders Compositions, syntheses, formulations and methods for treating or protecting the retina of a mammalian eye by contacting, with the retinal tissue, a therapeutically effective amount of retinyliden tauret (3,7-dimethyl-9-(2,6,6-trimehyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraen-1-imido-(N-ethane sulfonic acid)). The invention includes methods for synthesizing two (2) specific isomers of retinyliden tauret, namely (A) all-trans-[3,7-dimethyl-9-(2,6,6-trimehyl-1-cyclohexen- 1-yl)-2,4,6,8-nonatetraen- 1-imido-(N- ethane sulfonic acid)] and (B) 11-cis-[3,7-dimethyl-9-(2,6,6-trimehyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraen-1-imido-(N-ethane sulfonic acid)]. Also included are formulations and methods for administering such compounds to the retina of a mammalian eye to treat or prevent the progression or retinopathy.
CN102250075A 2,4-disubstituted quinazoline compounds and preparation method, medicinal composition and application thereof The invention discloses new 2,4-disubstituted quinazoline compounds and a preparation method, a medicinal composition and application thereof. The invention particularly relates to 2,4-disubstituted quinazoline compounds shown as a general formula I, medicinal salts thereof, precursors or derivatives thereof with the same biological function, a preparation method thereof, a composition containing one or more of the compounds, and application of the compounds in inhibiting activity of Pin1 enzyme, inhibiting activity of tumor growth and the like.
WO2009005045A1 Substituted dihydroisoquinoline derivative Disclosed are: a substituted dihydroisoquinoline derivative which can inhibit intracellular signaling or cell activation induced by an endotoxin or a cell response (e.g., the excess production of an inflammatory mediator) induced by the intracellular signaling or the cell activation, or a pharmacologically acceptable salt thereof; a pharmaceutical agent comprising the substituted dihydroisoquinoline derivative or the pharmacologically acceptable salt thereof as an active ingredient; a method for producing the substituted dihydroisoquinoline derivative or the pharmacologically acceptable salt thereof or the pharmaceutical agent; and a pharmaceutical agent useful for the prevention and/or treatment of a disease associated with intracellular signaling or cell activation induced by an endotoxin or a cell response induced by the intracellular signaling or the cell activation, such as sepsis (including septic shock, disseminated intravascular coagulation, multiple organ failure), which comprises the substituted dihydroisoquinoline derivative as an active ingredient. Specifically disclosed are: a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof; and a pharmaceutical agent comprising the compound as an active ingredient.
EP2176247A2 Derivatives of urea and related diamines, methods for their manufacture, and uses therefor The present invention relates generally to compounds represented in Formula (I), pharamaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.
CN103751188A Sodium cromoglycate, naphazoline hydrochloride and chlorpheniramine maleate nasal spray The invention provides a sodium cromoglycate, naphazoline hydrochloride and chlorpheniramine maleate nasal spray for treating allergic rhinitis. The sodium cromoglycate, naphazoline hydrochloride and chlorpheniramine maleate nasal spray comprises sodium cromoglycate, naphazoline hydrochloride, chlorpheniramine maleate, and pharmaceutically acceptable excipients, wherein the pharmaceutically acceptable excipients are selected from a buffering agent, an osmotic pressure regulator, a preservative, an absorption enhancer, a pH (Power of Hydrogen) regulator and the like. According to the sodium cromoglycate, naphazoline hydrochloride and chlorpheniramine maleate nasal spray, the active ingredients can be quickly absorbed through mucosa of nasal cavity and then acts quickly; the sodium cromoglycate, naphazoline hydrochloride and chlorpheniramine maleate nasal spray has the advantages of high bioavailability, outstanding compliance, and convenience in carrying and use, etc.
US7056918 Benzimidazole anti-inflammatory compounds The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; s is an integer from 0–5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
US20080139639 Proton Pump Inhibitors A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.
US20090233912 Non-aqueous pharmaceutical composition A composition for intranasal delivery of a drug comprising: includes: (i) the drug; and (ii) a non-aqueous vehicle containing (a) propylene glycol and at least one additional solvent selected from N-methylpyrrolidone, propylene carbonate, dimethyl sulfoxide and at least one propylene glycol fatty acid ester; (b) from about 40 to 100% by volume of N-methylpyrrolidone; or (c) from about 40 to 100% by volume of dimethyl sulfoxide (DMSO).
WO2009097973A2 Imidazopyridazines as par1 inhibitors, production thereof, and use thereof as medicaments The invention relates to compounds of formula (I) that have an antithrombotic activity and particularly inhibit protease-activated receptor 1 (PAR1), methods for the production thereof, and the use thereof as medicaments.
WO2009126931A3 Therapy for bipolar disorder and mania with buprenorphine Treatment regimens for mood disorders that include administration of buprenorphine, alone or in combination with additional pharmacological agents are described. Specifically, treatment regimens that alleviate racing thoughts associated with bipolar disorder, and pharmaceutical compositions and kits for use therein are described. Dosing regimens, compositions, and kits including buprenorphine for treating mania associated with opioid withdrawal are also described.
US7371820 Nutraceuticals for the treatment, protection and restoration of connective tissues The invention relates to a method for isolating from connective tissue a variety of glycosaminoglycan (GAG)-polypeptide complexes and polypeptides which are substantially free of contaminating DNA and other molecules such as viruses which may be associated with the DNA in the cell. The invention also relates to uses of GAG-peptide complexes and polypeptides substantially free of DNA either directly, or after further processing, for the treatment, protection and restoration of connective tissues in inflammatory and degenerative disorders such as rheumatoid arthritis and osteoarthritis in any of their multiple forms or other degenerative conditions in mammals.
CN103284963A Children calcium gluconate-milk composition freeze-dried oral disintegrating tablet and preparation method thereof The invention provides a children calcium gluconate-milk composition. The composition comprises the following ingredients in percentage by weight: 0.2-0.8% of calcium gluconate, 1.3-2.4% of mannitol, 2-4% of gelatin, 90-97% of milk powder, and 0.1-0.15% of sucralose. The invention also provides a children calcium gluconate-milk composition freeze-dried oral disintegrating tablet which is prepared from the composition. The freeze-dried oral disintegrating tablet is simple in ingredients, less in intestinal residue, complete in absorption, good in taste, and especially suitable for an infant to take, and does not need water and chewing when taken, and the disintegrating time of the freeze-dried oral disintegrating table in an oral cavity of a human body is not more than 2 seconds.
WO2008025820A1 Aminopyridine derivates as kinase inhibitors The invention relates to compounds of formula (I), wherein T1 and T2 have the meaning as cited in the description and the claims. Said compounds are useful as Itk protein kinase inhibitors for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
CN103405471A Compound preparation containing ilaprazole sodium The invention relates to the field of pharmaceutic preparations, in particular to a compound preparation containing ilaprazole sodium and a preparation method thereof. The preparation per unit is characterized by comprising 5-20 Mg ilaprazole sodium, 500-1500 sodium bicarbonate and suitable auxiliary materials. The invention also discloses a preparation method of the preparation. The preparation has the advantages of rapid onset and small side effect, and can be used for treating diseases such as hyperchlorhydria, gastroesophageal reflux disease, erosive esophagitis (short-term curative), active gastric ulcer, active duodenal ulcer (short-term curative) and the like.
EP1645556A1 Arylpiperazine-benzoylamide derivatives useful as pharmaceutical agents The invention relates to arylpiperazine-benzoylamide derivatives of formula (I) wherein A, X1, X2, n and R1 to R10 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation and the use thereof for preparing a pharmaceutical composition.
US20110171314 Non-viral compositions and methods for transfecting gut cells in vivo The present invention provides chitosan-based nanoparticles that can protect nucleic acids and deliver the same into gut mucosal cells. Compositions and methods for the expression of therapeutic nucleic acids in cells of the gut mucosa are provided. Compositions and methods for delivering therapeutic proteins systemically from cells of the gut mucosa are also provided.
CN102086211A Aromatic heterocyclic compounds serving as protein kinase inhibitor The invention provides a plurality of aromatic heterocyclic compounds, salt and pharmaceutically acceptable forms thereof, which are used for adjusting the activity of protein tyrosine kinase and the signal response among or in cells. The invention also relates to a composite which is pharmaceutically acceptable and comprises the compounds provided by the invention and a method for treating high-proliferation diseases of mammals by utilizing the composite, in particular to a method for the high-proliferation diseases of human.
CN102746259A Labdane diterpenoid compounds, arborvitae seed extract, preparation method thereof and application thereof The invention provides a plurality of labdane diterpenoid compounds and derivatives thereof, which can be used for preparing pharmaceutical composition for preventing or treating neurodegenerative diseases. The invention also provides an arborvitae seed extract, the arborvitae seed extract contains one or more labdane diterpenoid compounds and the derivatives, and can be used for preparing pharmaceutical composition for preventing or treating neurodegenerative diseases.
CN102440952A Iron-dextrin long-acting injection and preparation method thereof The invention relates to iron-dextrin long-acting injection and a preparation method thereof. The iron-dextrin long-acting injection is used for piglet iron supplement iron, and has the advantages that the release, absorption, distribution, metabolism and excretion processes of an iron preparation can be prolonged in vivo, so that the purpose of prolonging the action of a drug can be achieved, the number of the dosing times can be reduced, the complicance of livestocks is improved, the blood concentration can be stable, the peak and valley phenomena can be avoided, the side effects of the drug can be facilitated to be reduced, the total drug dosage is reduced, and further, the maximum drug effect by the minimum dosage is achieved. Thus, the iron-dextrin long-acting injection can completely play the role of long-acting iron supplement in the prevention and the cure of piglet iron-deficiency anemia.
CN103467484A Compound and medicine composition containing micronized prasugrel and salts of prasugrel The invention relates to a compound and medicine composition containing micronized prasugrel and salts of prasugrel. Prasugrel and the salts of prasugrel are micronized by adopting a superfine grinding technology till the particle sizes of the prasugrel and the prasugrel salts are in the range from 3micrometers to 10 micrometers, thus the micronized compound is obtained. The medicine composition is prepared from the micronized compound of prasugrel and the salts of prasugrel and appropriate auxiliary materials, wherein the weight of prasugrel and the salts of prasugrel accounts for 0.1%-10% of the total weight of the medicine composition. The superfine grinding technology is used for preparing the compound of the prasugrel and salts of the prasugrel and the particle size of the compound is 3 to 10 micrometers, so that the water solubility of the prasugrel and the prasugrel salts is increased, the biological availability is improved, and the clinical effect of the medicinal preparation is improved.
US20050287605 Caspase 3 inhibitors The invention is intended to develop a drug capable of directly or indirectly inhibiting the activation of caspase. Specifically, the invention provides a caspase 3 inhibitor comprising a protein comprising the same or substantially the same amino acid sequence as that represented by SEQ ID NO: 1, 2, 3 or 31 or a salt thereof. The protein of the invention, a partial peptide or a salt thereof is useful as a pharmaceutical such as a prophylactic and/or therapeutic agent for AIDS, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, pigmentary retinopathy, cerebellar degeneration, myelodysplastic syndrome, aplastic anemia, sideroblastic anemia, myocardial ischemia, conduction disturbance, chronic cardiac failure, graft-versus-host disease, or congenital or acquired enzymatic defect.
US20080255081 Antioxidant and radical scavenging activity of synthetic analogs of desferrithiocin Free radicals and reactive oxygen species have the potential to damage a wide variety of organic molecules, typically by oxidizing certain moieties. These damaging species can, for example, be produced by an organism as a by-product of cellular respiration or by the reaction of iron(II) and peroxide. The present invention includes methods of using aryl-substituted heterocyclic iron chelating compounds as antioxidants, as well as preventing the reduction of iron(III) to iron(II). In addition, the present invention provides methods of treating conditions such as inflammatory disease, neoplastic disease, and ischemic episodes.
WO2013082916A1 Strain of exopolysaccharide-secreting lactobacillus plantarum and application thereof Provided is a strain of exopolysaccharide-secreting Lactobacillus plantarum and an application thereof. The deposit number of the strain is CGMCC No. 5222. The strain differs from other strains of Lactobacillus plantarum in the amount of exopolysaccharide secreted, has unique physiological and biochemical characteristics and genetic background, and is a newly isolated and identified strain of Lactobacillus plantarum. The exopolysaccharide secreted by the strain is capable of eliciting B lymphocyte proliferation to enhance immunity, and is applicable in medicaments, healthcare products and food products for immunity enhancement.
WO2007118844A1 Substituted pyrazolopyrimidines, process for their preparation and their use for controlling harmful fungi and compositions comprising them Compounds of the formula (I) in which the substituents are as defined in the description. The invention further relates to fungicidal and pharmaceutical compositions comprising these compounds and to their use for controlling phytopathogenic fungi and cancer.
WO2013134558A1 Cancer treatment targeting non-coding rna overexpression Provided herein are methods directed to modulating the pro-oncogenic effects of noncoding RNAs (ncRNAs) through their interactions with specificity protein transcription factors (SpTFs). In one aspect, the disclosure provides a method of inhibiting growth of a cell, such as a transformed or cancer cell, characterized by overexpression of at least one specificity protein (Sp)-regulated ncRNA and expression of at least one Sp transcription factor (SpTF), the method comprising contacting the cell with an effective amount of an SpTF agent. In some embodiments, the ncRNA is a long noncoding RNA (IncRNA). In some embodiments, the ncRNA is a microRNA (miR). Also provided are methods of treating a cell proliferative disease, predicting the response of a subject to SpTF agent-based treatment, and monitoring the efficacy of a SpTF agent-based treatment in a subject.
US20080014154 Novel Ethylene Copolymers, Compositions Containing Said Copolymers and Treatment Method The invention relates to novel ethylene copolymers comprising 10-60% polyethylenglycol(meth)acrylate monomers and 40-90% substantially cationic monomer. Compositions, in particular cosmetic or pharmaceutical compositions, containing the inventive copolymers and a cosmetic treatment method using said copolymers are also disclosed.
CN102008476A Hydroxypropyl-beta-cyclodextrin inclusion of strychnine and preparation method thereof The invention discloses a hydroxypropyl-beta-cyclodextrin inclusion of strychnine and a preparation method thereof. The inclusion is prepared from the strychnine and hydroxypropyl-beta-cyclodextrin in weight ratio of 1: (1-100) by using the preferential inclusion process. Experimental results show that the hydroxypropyl-beta-cyclodextrin inclusion of the strychnine has the advantages of high inclusion rate, great drug loading and good stability, and can significantly improve the water solubility of the strychnine, lead the solubility in water to be more than 20 times that of the strychnine, significantly improve the bioavailability after administration of the strychnine, play a role in reducing the toxicity of the strychnine and lead the clinical application to be safer.
US20090275548 Compounds and methods for activated therapy Provided herein are compounds for detection, diagnosis and treatment of target tissues or target compositions, including hyperproliferative tissues such as tumors, using sonodynamic and/or photodynamic methods. In particular, photosensitizer and/or sonosensitizer compounds that collect in hyperproliferative tissue are provided.
EP2435049A1 Pharmaceutical composition comprising prostaglandin derivatives for use in modulating claudin mediated functions and in the treatment of dermatological disorders Disclosed is a pharmaceutical composition for modulating a claudin-mediated function in a mammalian subject which comprises administering to a subject in need thereof an effective amount of a specific fatty acid derivative. The application also discloses a method for treating a dermatological disease and a method for modulating an expression of a claudin in a mammalian subject using the same fatty acid derivative as above.
US20130216574 Kit providing multiple unmet therapeutic effects The present invention discloses a unique kit for providing a combinational therapeutic product comprising a medical device and a pharmaceutical composition to treat mammal diseases. The medical device is to meet these unmet needs of cleansing out these harmful substances, such as viruses, multiple drug resistant bacteria, fungi, pollen, dusts, or excessive mucus. The pharmaceutical composition adds the required functions of anti-inflammatory, anti-allergy, anti-cancer, promoting membrane healing or immunomodulating, to have the added effect of the medical device. The method of using the combinational product is also disclosed. The new product can be used to prevent and treat a variety of diseases, such as common cold, drug resistant influenza, sinusitis, post nasal drip, virus-triggered asthma, or chronic obstructive pulmonary disease. In addition, the new kit and the process of use are safe and cost effective.
CN102688252A Acarbose oral solid preparation composition and preparation method thereof The invention relates to the field of medicines, and discloses an acarbose oral solid preparation composition and a preparation method thereof. The acarbose oral solid preparation composition disclosed by the invention is composed of acarbose, a filler and a lubricant, wherein the powder flowability and compressibility of the acarbose oral solid preparation composition are greatly enhanced, and the prepared solid preparation is lower in moisture absorption and better in stability, and has a good industrial application prospect.
CN102218041A Ebastine solid dispersion and high-dissolubility ebastine tablet prepared by the same The invention provides an ebastine solid dispersion which comprises ebastine, poloxamer F68 and/or polyvinylpyrrolidone k30. The invention also provides a preparation method of the ebastine solid dispersion, and a high-dissolubility ebastine tablet. The method of the invention adopts poloxamer F68, polyvinylpyrrolidone k30 or a mixture of the two as a carrier, and prepares the solid dispersion by the carrier and ebastine; and the solubility of ebastine in water in the ebastine tablet is significantly improved. After accelerated tests and long-term tests, the dissolubility is stable without obvious changes.
EP1799198A1 Methods and compositions for the treatment of diseases characterized by pathological calcification Methods and compositions are provided which contains preparations of calcium chelators, bisphosphonates, antibiotics, antimicrobial agents, cytostatic agents, calcium ATPase and pyrophosphatase pump inhibitors, calcium phosphate-crystal dissolving agents, agents effective against calcium phosphate-crystal nucleation and crystal growth, and/or a combination of supportive agents and which may be used for treating and or reducing pathological calcifications, the growth of Nanobacteriu and calcification-induced diseases including, but not limited to, Arteriosclerosis, Atherosclerosis, Coronary Heart Disease, Chronic Heart Failure, Valve Calcifications, Arterial Aneurysms, Calcific Aortic Stenosis, Transient Cerebral Ischemia, Stroke, Peripheral Vascular Disease, Vascular Thrombosis, Dental Plaque, Gum Disease (dental pulp stones), Salivary Gland Stones, Chronic Infection Syndromes such as Chronic Fatigue Syndrome, Kidney and Bladder Stones, Gall Stones, Pancreas and Bowel Diseases (such as Pancreatic Duct Stones, Crohn's Disease, Colitis Ulcerosa), Liver Diseases (such as Liver Cirrhosis, Liver Cysts), Testicular Microliths, Chronic Calculous Prostatitis, Prostate Calcification, Calcification in Hernodialysis Patients, Malacoplakia, Autoimmune Diseases. Erythematosus, Scleroderma. Derrnatomyositis, Antiphospholipid Syndrome, Arteritis Nodosa, Thrombocvtopenia, Hemolytic Anemia, Myelitis, Livedo Reticularis, Chorea, Migraine, Juvenile Dermatomyositis, Grave's Disease, Hypothyreoidism, Type I Diabetes Mellitus. Addison's Disease, Hypopituitarism, Placental and Fetal Disorders, Polycystic Kidney Disease, Glomerulopathies, Eye Diseases (such as Corneal Calcifications. Cataracts. Macular Degeneration and Retinal Vasculature-derived Processes and other Retinal Degenerations. Retinal Nerve Degeneration, Retinitis, and Iritis), Ear Diseases (such as Otosclerosis, Degeneration of Otoliths and Symptoms from the Vestibular Organ and Inner Ear (Vertigo and Tinnitus), Thyroglossal Cysts, Thyroid Cysts, Ovarian Cysts, Cancer (such as Meningiomas, Breast Cancer, Prostate Cancer, Thyroid Cancer, Serous Ovarian Adenocarcinoma), Skin Diseases (such as Calcinosis Cutis, Calciphylaxis, Psoriasis, Eczema, Lichen Ruber Planus), Rheumatoid Arthritis, Calcific Tenditis, Osteoarthritis, Fibromyalgia, Bone Spurs, Diffuse Interstitial Skeletal Hyperostosis, Intracranial Calcifications (such as Degenerative Disease Processes and Dementia), Erythrocyte-Related Diseases involving Anemia, Intraerythrocytic Nanobacterial Infection and Splenic Calcifications, Chronic Obstructive Pulmonary Disease, Broncholiths, Bronchial Stones, Neuropathy, Calcification and Encrustations of Implants, Mixed Calcified Biofilms,.and Myelodegenerative Disorders (such as Multiple Sclerosis, Lou Gehrig's and Alzheimer's Disease) in humans and animals. The method comprises administering the various classes of compositions of the present invention, which together effectively inhibit or treat the development of calcifications in vivo.
EP2491027A1 Salts of imatinib with tartaric acids New imatinib acid addition salts are represented by general formula (I), wherein R represents O-acyl group of L- or D-tartaric acid, n represents any number in the range from 1 to 2, and their solvates and hydrates. Salts are preferably selected from a group comprising imatinib salts of dibenzoyl-L-tartaric, dibenzoyl-D- tartaric, di-p-anizoyl-L-tartaric, di-p-anizoyl-D-tartaric, di-p-tolyl-L- tartaric, dipivaloyl-L-tartaric or diacetyl-L-tartaric acids, which may be used in the treatment and/ or prevention of diseases mediated by tyrosine kinases.
US20090082420 Deuterium-enriched vildagliptin The present application describes deuterium-enriched vildagliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2009103032A1 Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases This invention is directed to compounds of formula (I): where, n, m, Y, R1, R2, R3, R4 and R5 are disclosed herein, as isolated stereoisomers or mixtures thereof, or as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising the compounds of formula (I); and methods of using the compounds and the pharmaceutical compositions in treating diseases or conditions associated with JAK2 activity.
US6858650 Stable salts of novel derivatives of 3,3-diphenylpropylamines The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products. The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(−)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.
US20080182854 4-Amino-5-Cyanopyrimidine Derivatives The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.
WO2012026665A1 Novel tacrolimus derivatives, a neuroprotective composition comprising the same, an immunosuppressive composition comprising the same, a method for preparing the same, and a mutant for producing the same The present invention relates to novel tacrolimus derivatives, a neuroprotective composition comprising the derivatives, an immunosuppressive composition comprising the derivatives, a method for producing the derivatives using a specific gene-deletion mutant, and a mutant for producing the derivatives. The novel tacrolimus derivatives, which are more excellent in neuroprotective and immunosuppressive effects than tacrolimus, can be efficiently produced by using the method of the present invention.
CA2355313C Controlled-release biocompatible ocular drug delivery implant devices and methods Controlled release devices are disclosed which are biocompatible and can be implanted into the eye. The devices have a core comprising a drug and a polymeric outer layer which is substantially impermeable to the entrance of an environmental fluid and substantially impermeable to the release of the drug during a delivery period, and drug release is affected through an orifice in the outer layer. These devices have an orifice area of less than 10% of the total surface area of the device and can be used to deliver a variety of drugs with varying degrees of solubility and or molecular weight. Methods are also provided for using these drug delivery devices.
CN1883497A Ginsenoside Rh2 hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof The invention provides a hydroxypropyl-beta-cyclodextrin inclusion compound of ginsenoside Rh2, wherein the ratio of ginsenoside Rh2 and hydroxypropyl-beta-cyclodextrin is 1:1-300. The invention also provides the process for preparing the inclusion compound and the preparations prepared from the inclusion compound.
US20120094946 Glycosylated chlorambucil analogs and uses thereof A library of glycosylated chlorambucil analogs which are useful as anti-tumor and/or anti-metastatic agents is disclosed. The glycosylated chlorambucil analogs have the general formula wherein represents a reducing sugar moiety.
US20100048695 Anti-fatigue agent Anti-fatigue agents containing dioxabicyclo[3.3.0]octane derivatives such as sesamin which is an ingredient contained in sesame, as well as pharmaceutical compositions and physiologically functional foods that contain such anti-fatigue agents are disclosed. These compounds can safely be administered to humans and animals alike and hence allow for continued ingestion while proving effective in promoting an improvement of stamina, an increase of body strength, a relief of fatigue, and recovery from fatigue.
CN102784162A Edible fungi compound polysaccharides health care treatment preparation The invention relates to an edible fungi compound polysaccharides health care treatment preparation which comprises the following raw materials according to part by weight: 50 to 150 parts of ganoderma polysaccharide, 50 to 150 parts of shii-take polysaccharide, 50 to 150 parts of Indian buead polysaccharide and 50 to 150 parts of boxthorn fruit polysaccharide. After the product is taken for a long time, the autoimmunity can be enhanced, a plurality of symptoms such as poor health, malnutrition, lassitude, fatigue, loss of appetite, dismay, choking sensation in chest of a cancer patient can be improved effectively, and harm caused by radiotherapy, chemotherapy and operations to the cancer patient can be relieved remarkably.
US8063051 9-substituted-8-oxo-adenine compounds as toll-like receptor (TLR7) modulators The present invention provides compounds of formula where n, R1, R2, A, X1, Y1, Z1, X2 and Y2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
CN1723894A Dripping pills contg. (R)-3-[(S)-(5-oxyl-2-pyrrolidinyl)carbonyl]- thiazolidine-4-carboxyl, and its prepn. method A dripping pill containing (R)-3-[(S)-(5-oxy-2-pyrrolidine) carboxyl]-thiazolidine-4-carboxyl (Piduomode) is prepared from (R)-3-[(S)-(5-oxy-2-pyrrolidine) carboxyl]-thiazolidine-4-carboxyl (Piduomode) and matrix through proportional mixing, dripping into cooling liquid and drying.
WO2011059294A3 Anticancer and immunity-enhancing composition containing morphinan alkaloids as active ingredients The present invention relates to an anticancer and immunity-enhancing composition containing morphinan alkaloids as active ingredients. In detail, the present invention relates to an anticancer and immunity-enhancing composition containing morphinan alkaloids as active ingredients, wherein the morphinan alkaloids are separated from Stephania delavayi Diels, and have the following chemical formula. The separated and purified morphinan alkaloids of the present invention inhibit the proliferation of cancer cells, induce apoptosis, suppress the progression of a cell cycle, and inhibit the growth of tumors, thus exhibiting superior anticancer activity. The morphinan alkaloids of the present invention have immunomodulating and immunity-enhancing effects, and have no toxicity or side effects, and therefore can be used as materials for medicine for preventing or treating cancer and materials for functional health foods for enhancing immunity.
US20100239687 Uses of rare earth elements for slimming Disclosed is a use of rare earth element selected from the group consisting of lanthanum (La), cerium (Ce), praseodymium (Pr), neodymium (Nd), promethium (Pm), samarium (Sm), europium (Eu), gadolinium (Gd), terbium (Tb), dysprosium (Dy), holmium (Ho), erbium (Er), thulium (Tm), ytterbium (Yb), lutetium (Lu), scandium (Sc) and yttrium (Y), and a mixture thereof, or a salt or an oxide, for promoting lipidolysis, anti-cellulite, enhancing skin firmness, or for slimming.
WO2014076235A1 Modulators of intracellular chloride concentration for treating fragile x syndrome The present invention relates to a composition for treating Fragile X syndrome in a subject in need thereof, wherein said composition comprises an effective amount of a modulator of a chloride transporter.
US20080262056 (S) N-[3-(1-methyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide; staphylococci, streptococci, Enterococci, Haemophilus, Moraxella, bacteroides, clostridia, Mycobacteria, or Chlamydia The present invention relates to novel oxazolidinones derivatives of oxindoles of formula I or a pharmaceutically acceptable salt thereof wherein: Y1 is CH or CF; R1 is —C1-4alkyl, optionally substituted with a fluoro atom, or R1 is —C3-5cycloalkyl; and R2 is —C1-2alkyl. These compounds are useful as antibacterial agents.
EP2711009A1 Compounds for use in treating or preventing primary and metastatic breast and prostate cancer The present invention relates to the field of biotechnology. The present invention relates to a compound of formula (I) for use in the treatment or prevention of primary and metastatic breast and prostate cancer. The present invention also relates to a combination of a compound of formula (I) with at least one further compound for use in the treatment or prevention of primary and metastatic breast and prostate cancer. The present invention further relates to a pharmaceutical composition comprising the compound of formula (I) or the combination.
CN1842594A Inhibition of apoptosis-specific elF-5A ('elF-5Al') with antisense oligonucleotides and siRNAs as anti-inflammatory therapeutics The present invention relates to apoptosis specific eucaryotic initiation factor 5A (eIF-5A), referred to as apoptosis-specific eIF-5A or eIF5A1, nucleic acids and polypeptides and methods for inhibiting or suppressing apoptosis in cells using antisense nucleotides or siRNAs to inhibit expression of apoptosis-specific eIF-5A. The invention also relates to suppressing or inhibiting expression of pro-inflammatory cytokines or inhibiting expression of pro-inflammatory cytokines or inhibiting activation of NFkB by inhibiting expression of apoptosis-specific eIF-5A.
CN102058529A Oral liquid slow-release preparation containing ondansetron and preparation method thereof The invention discloses an oral liquid slow-release preparation containing ondansetron and a preparation method thereof. The preparation comprises ondansetron, ion exchange resin, a hydrophilic or water soluble material, a coating material, a plasticizer, a suspending agent, a metal ion complexing agent, a surfactant, a preservative, a flavoring agent and deionized water. The ondansetron is absorbed on the ion exchange resin to form particles externally coated with the coating material and the medicated resin coating particles are distributed uniformly in a liquid medium of the suspending agent and the deionized water in a suspension manner. The preparation method comprises the steps of preparing the medicated resin, coating the medicated resin and preparing the medicated resin suspension. Compared with prior art, the invention has the advantages of obvious slow-release effect, reduced frequency of taking, good taste and great convenience for medication of patient in chemotherapy.
US20090118298 Octahydropentalene compounds as chemokine receptor antagonists The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.
WO2013060258A1 Clavatine a-c, preparation method thereof and pharmaceutical composition and use thereof The present invention relates to 3 alkaloids (clavatine A-C) isolated from Lycopodium japonicum Thunb., a pharmaccodynamically acceptable salt thereof and a preparation method thereof, a pharmaceutical composition containing this class of compounds and the use of this class of compounds in preparing acetylcholinesterase inhibitor drugs, drugs for treating Alzheimer's disease and drugs for resisting diseases related to decline in memory and cognitive ability of middle-aged and elderly people.
WO2008028914A1 Combination treatment for diabetes mellitus The invention relates to combinations of (2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8- methoxy-1,2,3,4,4a,10b-hexahydrophenanthridin-2-ol with other active compounds for the treatment of diabetes mellitus type 2 and/or type 1.
CA2435714C Fenofibrate tablets The present invention relates to a galenic formulation of fenofibrate for oral administration and to the process for its preparation. According to the invention, the formulation is a tablet obtained by compressing a mixture comprising: a) granules containing:- 1 to 5% of a surfactant;- micronized fenofibrate; and - at least one solid excipient selected from starch, cellulose and derivatives thereof, with the exception of C12 disaccharides, said granules being obtained by granulating the mixture with the aid of an aqueous solution of polyvinylpyrrolidone;b) crosslinked polyvinylpyrrolidone; and c) optionally flow aids or lubricants, the amount of fenofibrate being greater than 50% by weight, expressed relative to the weight of the tablet. The formulation in accordance with the invention is useful in the treatment of hypercholesterolemia and hypertriglyceridemia.
WO2010117323A1 Method and apparatus for producing heat energy and carbon dioxide Formula I or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.
US8614330 Substituted benz-azoles and methods of their use as inhibitors of RAF kinase New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
US20110071217 Process for the Synthesis of 4,5,6,7-tetrachloro-3',6'-dihydroxy-2',4',5',7'-tetraiodo-3H-spiro[isobenzofuran-1,9'-xanthen]-3-one (Rose Bengal) and Related Xanthenes A new process for the manufacture of iodinated xanthenes in high purity includes a cyclization step followed by an iodination step. No extraction, chromatographic or solvent concentration steps are required, and the intermediate as well as final compounds are isolated via filtration or similar means. The process requires a single organic solvent, and the steps are completed at temperatures below 100° C. The exclusion of chloride ions, of chloride free-radicals, hypochlorite ions, or hypochlorous acid as reagents or from reagents that may generate these species in situ in the presence of oxidants, prevents undesirable impurity formation. Several new compounds have been conceived and isolated using these methods. These new compounds are also formed into new medicaments.
EP2116542A1 Solid of macrolide compound, method for production thereof, and pharmaceutical composition comprising the same The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.
US20110243854 Methods and systems for identifying modulators of longevity Methods of treating disorders such as neurofibromatosis-1 are provided, including methods in which catalytic antioxidants such as metalloporphyrins are administered. Methods of regulating longevity, and methods and systems for screening for modulators of aging or longevity, are also provided. In addition, related transgenic animals are described.
US20080299125 Genetic basis of treatment response in depression patients The invention provides a collection of polymorphic sites associated with response to treatment by an SSRI or placebo in depression patients. The polymorphic sites and others in linkage disequilibrium with them are useful in determining whether to treat a patient with an SSRI or include a patient in a clinical trial to test an SSRI.
US20090156672 Substituted Phenyl Aziridine Precursor Analogs as Modulators of Steroid Receptor Activities Disclosed are methods and pharmaceutical compositions for modulating one or more steroidal receptor activities. The methods typically utilize and the pharmaceutical compositions typically include one or more substituted phenyl aziridine precursors, their respective aziridines, analogs thereof, derivatives thereof, or pharmaceutically acceptable salts thereof such as CpdA. The methods and compositions may be used for treating diseases, disorders, and conditions associated with glucocorticoid receptor activity, androgen receptor activity, or both, such as cancers, acne vulgaris, and alopecia.
CN1989976A Effective therapeutic agent for ringworm of the nails The invention relates to a medicament for treating ringworm of the nails, wherein the medicament is prepared mainly from 2-hydroxybenzoic acid, benzene carboxylic acid, thymol, propanone and tincture of iodine (7%) through specific processes.
CA2634811C Novel modifications to 2-amino-4-(4-fluorobenzylamino) -1- ethoxycarbonyl-aminobenzene and processes for preparing said compound The invention concerns novel modifications to the compound 2-amino-4-1-ethoxycarbonyl-aminobenzene of formula. The invention also concerns processes for preparing this compound and its use in pharmaceutical compositions.
CN101066284A Medicine for treating mycotic colpitis The present invention relates to medicine, and is especially one kind of medicine for treating mycotic colpitis. The medicine consists of 1 vaginal lactic acid bacteria capsule in 0.25 g weight and containing 6 million live lactic acid bacteria, and 1 clotrimazole tablet in 0.15 g weight. It is prepared through crushing clotrimazole tablet, mixing with live lactic acid bacteria from 1 vaginal lactic acid bacteria capsule, encapsulating the mixture, and cold storing. It can eliminate harmful bacteria, replenish beneficial bacteria, balance micro ecoenvironment and heal mycotic colpitis radically.
WO2010146025A1 Tricyclic azabicyclo [4.1.0] heptane derivatives as inhibitors of serotonin, dopamine and norepinephrine re-uptake The invention relates to compounds of formula (I), processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
US20120065251 Mir-21 promoter driven targeted cancer therapy The invention provides a nucleic acid construct comprising a promoter sequence derived from microRNA-21 (miR-21) linked to a nucleic acid sequence encoding an anti-cancer agent, an example of which is a toxin. The constructs of the invention are particularly useful for treating tumors expressing miR-21.
US6949506 Relaxin-like factor and methods and uses thereof The present invention relates to a relaxin-like factor, its derivatives or analogs, and uses thereof. The present invention further relates to compositions comprising a relaxin-like factor, its derivatives or analogs, and relaxin wherein such composition exhibits an additive or synergistic effect.
EP1603499A2 Invisible patch for the controlled delivery of cosmetic, dermatological, and pharmaceutical active ingredients onto the skin The present invention relates to a patch for controlled topical or transdermal delivery of effective levels of cosmetic, dermatological, and pharmaceutical active ingredients onto the skin, hair follicles, and sebaceous glands, with minimal discomfort and ease of use. The patch can be transparent or clear and comprises a rate-controlling matrix layer. The matrix layer comprises water-sensitive, bioadhesive, film forming polymers, a water soluble oligomer, and a surfactant. The cosmetic, dermatological, and pharmaceutical active ingredients are soluble or dispersed in the matrix. The patch becomes tacky when wetted and adheres onto the skin. The adhesive properties of the patch are sufficient to maintain the patch in place on the skin for the recommended treatment period while allowing the patch to be readily removed without causing skin irritation or leaving adhesive residue on the skin.
WO2011112893A2 Compositions for ameliorating cell proliferative disorders and methods of making and using them In alternative embodiments, the invention provides apratoxin F and apratoxin G compounds, which include apratoxin F and apratoxin G stereoisomers, derivatives and analogs compositions and methods. In alternative embodiments, the invention provides pharmaceutical compositions and formulations comprising apratoxin F (compound 6 of Figure 1) and apratoxin G (compound 7 of Figure 1) and their stereoisomers, derivatives and analogs. In alternative embodiments, pharmaceutical compositions and formulations of the invention are administered in an amount sufficient to treat, prevent and/or ameliorate a disease or condition that can be ameliorated by decreasing or inhibiting cell growth, e.g., pathological, uncontrolled or unwanted cell growth, e.g., a cancer or a metastases, or any disease or condition (e.g., allergy) or infection having a hyperproliferative cell growth component.
CN1823790A Preparation method of bacteriostatic agent sulfadiazine cerium A process for preparing the sulfapyrimidine cerium used as bacterial depressant for promoting the healing of wound and preventing residual scar is prepared through dissolving sodium hydroxide in deionized water, adding sulfapyrimidine to obtain solution A, dissolving cerium nitrate in deionized water to obtain solution B, dripping the solution B in A, reaction to generate the deposit of sulfapyrimidine cerium, washing, drying in the air, pulverizing and sieving.
US20080063620 biodegradable amphiphillic copolymers comprising hydrophobic and hydrophillic segments, capable of undergoing transitions that results in an increase in viscosity in response to a change in temperature, used for drug delivery, prevention of surgical adhesions, as bioadhesives and in tissue engineering The invention provides a responsive polymeric system, comprising: a polymeric responsive component capable of undergoing a transition that results in a sharp increase in viscosity in response to a change in temperature at a predetermined body site; wherein the polymeric component comprises hydrophilic and hydrophobic segments covalently bound within the polymer component, by at least one chain extender or coupling agent, having at least 2 functional groups; wherein the hydrophilic and hydrophobic segments do not display Reverse Thermal Gelation behavior of their own at clinically relevant temperatures and; wherein the viscosity of the polymeric component increases by at least about 2 times upon exposure to a predetermined trigger.
EP0710116B1 Prevention and treatment of pathologies associated with abnormally proliferative smooth muscle cells TGF-beta activators and TGF-beta production stimulators are employed to maintain or increase vessel lumen diameter in a diseased or injured vessel of a mammal. Conditions such as restenosis following angioplasty, vascular bypass grafts, transplanted organs, atherosclerosis or hypertension are characterized by a reduced vessel lumen diameter. In a preferred embodiment of the invention, TGF-beta activators and production stimulators inhibit abnormal proliferation of smooth muscle cells. TGF-beta activators or production stimulators that are not characterized by an undesirable systemic toxicity profile at a prophylactic dose are also amenable to chronic use for prophylactic purposes with respect to disease states involving proliferation and/or migration of vascular smooth muscle cells over time. Further provided is a method for determining TGF-beta in vitro, thereby identifying a patient at risk for atherosclerosis and monitoring a recipient that has received one or more administrations of a TGF-beta activator or production stimulator.
CN102038651A Ropivacaine mesylate freeze-dried powder injection The invention relates to a ropivacaine mesylate freeze-dried powder injection which consists of ropivacaine mesylate and a PH regulator and is prepared by using the following freeze drying method: (1) a section quick-freezing stage: keeping bulked ropivacaine mesylate solution at the temperature of 0 DEG C for 10-30 minutes, and then keeping the bulked ropivacaine mesylate solution at the temperature of minus 35 DEG C-minus 45 DEG C for 1-2 hours; (2) a lyophilization stage: heating to 0 DEG C under the vacuum degree of 10-20 Pa and at the speed of 2-10 DEG C/h, and then keeping the temperature for 1-3 hours; and (3) a desorption drying stage: heating to 30 DEG C under the vacuum degree of 0-10 Pa and at the speed of 5-10 DEG C/h and keeping the temperature for 2-5 hours. The freeze-dried powder injection provided by the invention has the advantages of high yield, good re-dissolubility, more stable quality and the like.
CN101288674A New dosage medicinal application and using method of adefovir dipivoxil The invention provides the application of a preparation, each unit of which contains 12-20mg of adefovir dipivoxil, in preparing the medicine for treating hepatitis B virus disease infected by patients who are 20 to 50 years old, have more than 50kg body weight and no less than 55 ml/min creatinine clearance rate in renal function measurement indicators. The dosage form is a tablet or capsule orally taken once a day and the continuous treatment time can not exceed 18 months.
EP1836168B1 Benzoyl-tetrahydropyridine as glyt-1 inhibitors The present invention relates to compounds of the general formula (I); Wherein R1 is a non aromatic heterocycle or OR'; R’ is lower alkyl, lower alkyl substituted by halogen or is -(CH2)n-cycloalkyl; R2 is NO2, CN or SO2R'; R' is lower alkyl; Ar is phenyl, optionally substituted by halogen, cyano, lower alkyl substituted by halogen or SO2 R '; n is 0, 1 or 2; and to pharmaceutically active acid addition salts and to there use in the treatment of neurological and neuropsychiatry disorders.
CN101365695A Quinazoline derivatives as anticancer agents A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man.
US20110257225 Cyclohexylamine derivative containing phenyl group, and therapeutic agent for diseases accompanied by central nervous system disorders Disclosed is a novel cyclohexylamine derivative containing a phenyl group, which is useful as a novel sigma receptor ligand. Also disclosed is a therapeutic agent for diseases accompanied by a central nervous system disorder, which comprises the compound as an active ingredient. The therapeutic agent comprises a compound represented by general formula [1] or a pharmacologically acceptable salt thereof as an active ingredient: wherein X and Y independently represent a hydrogen atom, a halogen atom, a trihalomethyl group, a dihalomethyl group, a monohalomethyl group, a methoxy group, a hydroxyl group, or an alkyl group having 1 to 3 carbon atoms; R1, R2, R3 and R4 independently represent a hydrogen atom, a hydroxyl group, an alkoxyl group having 1 to 3 carbon atoms, or an alkyl group having 1 to 3 carbon atoms; R5 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, or an alkylene group which has 2 to 4 carbon atoms and can bind to a carbon atom other than carbon atoms that bind to a nitrogen atom on the cyclohexyl ring to form a ring; n represents an integer of 1 to 5; and Z represents a sulfur atom, a carbon atom, or an oxygen atom.
WO2010004016A1 Use of phenoxyalkylamines in cosmetic and/or dermatological compositions The invention relates to the use of compounds of the phenoxyalkylamine family of formula (I) in cosmetic and/or dermatological compositions, especially as preserving agents. The invention also relates to compositions comprising, especially as preserving agent, at least one phenoxyalkylamine of formula (I). The invention also relates to particular compounds of the phenoxyalkylamine family of formula (I) and to cosmetic and/or dermatological compositions containing them.
CN100584383C Pharmaceutical composition with Meclofenoxate hydrochloride capable of preventing hydrolysis The invention relates to an alcaine methyl chloroformate compound which can avoid hydrolysis. Wherein, said compound comprises active component alcaine methyl chloroformate, findings, lubricant and stabilizer, while the stabilizer can keep the compound at weak acid. And the invention uses full powder compress method to avoid hydrolysis problem.
US7078437 suppressing degradation of apolipoprotein D to prevent schizophrenia or other diseases caused by denaturation or cell damage in the nervous system, such as Alzheimer's disease, Niemann-Pick disease type C and Unverrichit-Lundborg disease by administering lauric acid or oleic acid The invention contemplates drugs useful for maintenance or promotion at sites of regenerating nerves and for prevention or treatment of pathological conditions caused by denaturation or cell damage in the nervous system. Thus, the invention provides an apolipoprotein D degradation inhibitor containing lauric acid or oleic acid as an active ingredient.
WO2012085654A1 Novel anti-tuberculosis agents Novel benzothiazinone derivatives of formula (I) or a pharmaceutically acceptable salt or solvate thereof have been found to be effective against Mycobacterium tuberculosis strains and may thus be useful in the treatment of tuberculosis (I) wherein, EWG (electron withdrawing group) = N02, CN, CF3, F, CI, Br, OCF3, OH, OR, OCHF2, COOR, wherein R is hydrogen, or a straight or branched C1-C4 alkyl group, X = a bond, or a straight or branched C1-C4 alkylene group; Y = a bond, or a straight or branched C1-C4 alkylene group; wherein either one of X or Y is a bond and the other is a Ci-C4-alkylene group, Z = N or C, n = 1 or 2; R1 = hydrogen, a straight or branched C1-C6 alkyl group, or a C3-C6 cycloalkyl group, which may be substituted with a group selected from F, CI, Br, I or a C1-C4 alkoxy; R2 = a phenyl group, a naphthyl group or a thienyl group, each of which may be unsubstituted or substituted with one or more substituent(s) which may be the same or different from each other, selected from the group consisting of F, CI, Br, I, CN, NO2, or a straight or branched C1-C6 alkyl or phenyl group, which may be substituted with a group selected from F, CI, Br, I, or C1-C4 alkoxy.
CN1596890A Medicine having antivirus action An antivirus medicine features that its active components are arginine, dewatered andrographolide and semi-succinate derivative.
WO2007068905A1 1,2,4-TRIAZOL-l-YL BISPHENYL DERIVATIVES FOR USE IN THE TREATMENT OF ENDOCRINE-DEPENDENT TUMOURS There is provided a compound of Formula I wherein R3, R4, R5, R6 and R7 are independently selected from H and -Y-R6; wherein each R8 is independently selected from -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO2), H-bond acceptors, and halogens; wherein at Jeast one of R3, R4, R5, R6 and R7 is -Y-R8 wherein R8 is selected from substituted and unsubstituted • heterocyclic rings and amino substituted phenyl groups, wherein X is a bond or a linker group; wherein Y is an optional linker group; and wherein ring A is optionally further , substituted; wherein R9 is selected from H, -OH and -OSO2NR1R2; wherein R1 and R2 are independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R3, R4, R5, R6 and R7 is -Y-R8; OR (b) R9 is -OSO2NR1R2 or - OH and four of R3, R4, R5, R6 and R7 are H and one of R3, R4, R5, R6 and R7 is -Y-R8. These compounds inhibit steroid sulphatase and aronatase activity and are useful in the treatment of endocrine-dependent tumours.
US7550449 4-(alkylcarbonyloxymethyl)-2-oxo-2-methoxy-1,2-oxaphospholane; anticancer, antimetastasis agents It is an object of the present invention to synthesize a carba cyclic phosphatidic acid derivative having a novel structure by substituting O at position sn-2 of the glycerol skeleton with CH2, and study the action of the obtained derivative to suppress cancer cell invasion. The present invention provides a compound represented by the following formula (I): wherein R represents a linear or branched alkyl group containing 1 to 30 carbon atoms, a linear or branched alkenyl group containing 2 to 30 carbon atoms, or a linear or branched alkynyl group containing 2 to 30 carbon atoms, wherein these groups may comprise a cycloalkane ring or aromatic ring; and M represents a hydrogen atom or counter cation.
WO2012075026A1 Methods of treating obesity using an effective dose of a metap-2 inhibitor The invention generally relates to methods of treating an overweight or obese subject, and treating overweight- or obesity-related conditions using effective of amounts of a MetAP-2 inhibitor.
CN103356986A Spleen-warming and diarrhea-stopping pills, and preparation method thereof The invention relates to spleen-warming and diarrhea-stopping pills, and a preparation method thereof. The pills comprise the components of, by mass: 20-30 parts of sharpleaf galangal fruit, 5-13 parts of malaytea scurfpea fruit, 13-30 parts of medicine terminalia fruit, 4-10 parts of fennel, 15-25 parts of largehead atractylodes rhizome, 15-25 parts of dried ginger, 4-10 parts of dodder, 10-18 parts of common yam rhizome, 5-12 parts of canton abrus herb, 2-6 parts of agaric, 2-6 parts of red halloysite, 13-30 parts of pomegranata rind, 32-64.5 parts of microcrystalline cellulose, and 16-32.3 parts of honey. The spleen-warming and diarrhea-stopping pills provided by the invention have significant treatment effect in treating splenasthenic diarrhea, and have good taste. With the pills, body immunity can also be improved.
US20090092590 Method for improving stool characteristics in infants In accordance with the present invention, a novel method for improving the stool characteristics, reducing the incidence of diarrhea, and firming the stool of a formula-fed infant of a formula-fed infant has been discovered. The method comprises administering to the infant at least one prebiotic and hydrolyzed pectin.
US6992189 Such as 4-((Z)-(4-bromophenyl)(ethoxyimno)methyl)-1'-((2,4-dimethyl-1-oxido-3-pyridinyl)carbonyl)-4'-methyl-1,4'-bipiperidine; for the treatment of AIDS and related HIV infections In its several embodiments, this invention discloses novel processes to prepare the compounds of formula II and formula IV:
US7803840 Use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets; dimethyl fumarate The present invention relates to the use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets. For this purpose, the dialkyl fumarates may also be used in combination with conventional preparations used in transplantation medicine and immunosuppressive agents, especially cyclosporines.
CN102198131A New compound preparation containing omeprazole The invention relates to a new compound preparation containing omeprazole, and the compound preparation is characterized by comprising omeprazole, dihydroxyaluminium aminoacetate, and pharmaceutical excipients. Wherein, dihydroxyaluminium aminoacetate has the direct effect of inhibiting gastric acid secretion and the function of preventing the degradation of omeprazole by gastric acid. Thus the preparation is reasonable in composition. When the preparation is taken, drug absorption is rapid, and a peak concentration can be reached rapidly, so that gastric acid can be effectively controlled. Compared with traditional omeprazole preparations added with sodium bicarbonate, the compound preparation provided in the invention has the characteristics of small dosage of gastric acid secretion inhibitor, lasting effect, no aerogenesis, and inabsorbability in the human body.
CN101590033A Medicinal composition fat emulsion injection containing eucalyptol, limonene and alpha-pinene and preparation method The invention aims to develop medicinal composition fat emulsion injection containing eucalyptol, limonene and alpha-pinene and a preparation method. The preparation comprises the following components in percentage by weight: 0.0128 to 0.0320 percent of eucalyptol, 0.0084 to 0.0210 percent of limonene, 0.0028 to 0.0070 percent of alpha-pinene, 10 to 30 percent of soybean oil for injection, 1.0 to 1.5 percent of yolk lecithin for injection or 0.8 to 1.5 percent of soybean phospholipids for injection, 2.0 to 2.5 percent of glycerol for injection, and water for injection added to 100 milliliters. The preparation method has the characteristics of strong controllability of production quality, and definite treatment effect of a product. The invention fills up the blank of the medicinal composition fat emulsion injection preparation containing the eucalyptol, the limonene and the alpha-pinene.
WO2012020795A1 Nucleic acid/polysaccharide complex The purpose of the present invention is to provide a highly stable nucleic acid/polysaccharide complex consisting of an siRNA and sizofiran. The nucleic acid/polysaccharide complex is formed by adding polydeoxyadenine, at least a part of the phosphodiester bond moieties of which has been converted into phosphorothioate, to an siRNA and then forming a complex with sizofiran.
CN101157718B Triterpenoid saponins antineoplastic compound griseaside A in ash sea cucumber and preparation method thereof The present invention relates to the field of pharmaceutical technology, in particular to an anti-tumor compound of triterpenoid saponins (the molecular formula is C60H96O28) which is separated from the gray sea cucumbers and is named as griseaside A, a chemical structure is as the right, the chemical structure and a spatial configuration of the compound are determined by a plurality of modern spectral analyses, particularly by a plurality of advanced two-dimension nuclear magnetic resonance spectroscopy comprehensive analyses. The in vitro anti-tumor tests show that the compound has significant inhibiting effect for four tumor cell strains of A-549 human gastric carcinoma cells, HL-60 human acute promyelocytic leukemia, Molt-4 human T lymphocyte leukemia cells and BEL-7402 human hepatoma cells, etc. The present invention can provide a lead compound for the development of new anti-tumor drugs and has important value for the development and utilization of marine medical resources.
US20080261970 metabolic syndrome; diabetes; obesity; N-(2-(benzyloxy)-1-(6-methyl-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-1-methylpiperidine-4-sulfonamide Compounds of formula (I), including methods of making and methods of using are described in formula (I).
US7339064 Benzimidazole compound crystal A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.
CN1985950A Slow released capsule of cefotaxime sodium and bletilla tuber glue for animal and birds The present invention belongs to the field of veterinary medicine technology, and is especially slow released veterinary medicine capsule prepared with cefotaxime and bletilla tuber as material. The preparation process includes the following steps: water extracting and alcohol precipitation to extract bletilla tuber glue; mixing cefotaxime and bletilla tuber in the ratio of 1 to 3 and 10 % concentration alcohol solution of PVP as adhesive; making pellet of 20 meshes and encapsulating. The slow released veterinary medicine capsule has long medicine retaining time in the disease focus, high local medicine concentration, excellent bioadhesion and obvious medicine slow releasing characteristic.
CN102766083A 2-amino-3-perfluoro acetoindole compound and its derivative, preparation method and application thereof The invention discloses a 2-amino-3-perfluoro acetoindole compound and its derivative, a preparation method and an application thereof. The compound has the chemical structural general formula defined in the specification, wherein R represents a monosubstituent, a disubstituent, a trisubstituent or a tetrasubstituent on a phenyl ring. The substituent is H, F, Cl, Br, nitro or C1-C3 alkyloxy. The derivative has the chemical structural general formula defined in the specification, wherein R is the same as mentioned above; and R1 is acetonyl, C1-C4 alkyl or C1-C4 nonsaturated alkyl. The compound is prepared by a reaction between the 2-amino-3-perfluoro acetoindole compound and trifluoroactic anhydride. The derivative is prepared by a reaction between the 2-amino-3-perfluoro acetoindole compound and a Grignard reagent or acetone. The 2-amino-3-perfluoro acetoindole compound and its derivative provided by the invention can be applied as an HIV reverse transcriptase inhibitor.
WO2014145095A1 Macrocyclic and bicyclic inhibitors of hepatitis c virus Compounds of formula (I):or pharmaceutically acceptable salts thereof, wherein the various substituents are defined herein, methods of using said compounds, and pharmaceutical compositions containing said compounds.
US20120141505 Cd19-ligand and use Provided herein are CD19-ligand (CD19-L) polypeptides and polynucleotides encoding such CD19-L polypeptides. Methods related to diagnosing and treating a disorder associated with CD19 positive B-cells in a patient using a CD19-L polypeptide are also provided.
WO2006107923A1 Substituted benzylimidazoles useful for the treatment of inflammatory diseases The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory conditions.
US8492366 E.g., salicylic acid, containing an alpha-hydroxy acid such as lactic, glycolic or citric acid The solubility in solvent media, notably alcoholic media, of the beta-hydroxy acids (“BHAs”), notably the chemical skin peeling agent salicylic acid, is markedly enhanced by solubilizing same in the presence of at least one alpha-hydroxy acid (“AHA”); higher potency, more concentrated BHA skin peel products are thus formulated.
US20080260735 Glycoprotein-340 for use in targeted destruction of cancer tissues; immunotherapy The present invention provides a humanised form of the antibody 340 obtainable from the cell line deposited with the ECACC under accession number 97021428. Such antibodies have been found to have an increased ability to kill cells compared to the murine antibody 340. Also provided are nucleic acids encoding such antibodies, as well as the use of the antibodies in medicine, in particular in the treatment of cancer.
CN102018744A Formula for treating hiccough The invention discloses a formula for treating hiccough, which consists of the following components in percentage by weight: 25 to 30 percent of calyx and receptacle of persimmon, 25 to 30 percent of silkworm cocoon, 10 to 15 percent of costus root and 25 to 30 percent of brown sugar. A method for preparing the formula for treating the hiccough comprises the following steps of: decocting 25 to 30 percent of calyx and receptacle of persimmon, 25 to 30 percent of silkworm cocoon and 10 to 15 percent of costus root in water for 5 to 15 minutes; filtering off dregs; and adding 25 to 30 percent of brown sugar, stirring and storing in a container for administration according to dosage. The invention has the advantage that: the formula for treating the hiccough is particularly suitable for weak patients.
CN102526025A Method for preparing ginkgo leaf extractive containing a plurality of appointed active ingredients The invention relates to a method for preparing a ginkgo leaf extractive containing a plurality of appointed active ingredients, which comprises the following steps of: firstly extracting the active ingredients of ginkgo by using ginkgo leaves or a ginkgo leaf extractive, extracting a ginkgo flavone containing part of an intermediate I, further extracting ginkgo lactone A, ginkgo lactone B and ginkgo lactone C parts of an intermediate II, then extracting a ginkgo lactone part of an intermediate III, weighing the ginkgo flavone containing part, the ginkgo lactone A, ginkgo lactone B and ginkgo lactone C parts and the ginkgo lactone part according to the standard required contents, and then directly mixing or mixing with the ginkgo leaf extractive with the content not meeting the requirement to obtain the ginkgo leaf extractive meeting the requirement of the specified standard, such as EP6.0 standard or USP31 standard or the requirement appointed by clients. The method makes up the defects that due to the combined action of various factors on the quality of the ginkgo leaves, such as producing areas, weathers, ages of trees, collecting times, storage periods and the like, the extractive has unstable quality, the relative stability and accuracy of flavones and lactone contents, the proportion of total flavone and total lactone and the proportion of ginkgo lactone A, ginkgo lactone B and ginkgo lactone C parts and the ginkgo lactone part are difficultly ensured, and has the characteristics of low requirement of raw materials, easiness in production control and accuracy and stability in active ingredient content of the prepared product.
US7354736 Intracellular caspase inhibitory polypeptide for use in treatment and prevention of cell proliferative, nervous system and autoimmune disorders The present invention relates to a caspase-8 interacting polypeptide (Cari), methods for its preparation, and its use.
US20080280956 Heteroarylsulfonyl Stilbenes as 5-Ht2a Antagonists Compounds of formula I: are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various 10 CNS disorders.
WO2014006414A1 Polymorphs of|n-[(r)-1 -[(s)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoy l]-2-(4-e|thoxy-phenyl)-ethyl]-benzamide hydrochloride The invention provides new polymorphs of N-[(R)-l-[(S)-l-(4-aminomethyl- benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride, pharmaceutical compositions containing them and their use in therapy.
EP1370276B1 Intercellular communication facilitating compounds and their medical use Disclosed are novel peptides including antiarrhythmic peptides that have improved stability. Further disclosed are compositions that include such peptides and methods of using the compositions particularly as medicaments.
CA2602396C Alkyl sulfate free and orthophosphate free dentifrice composition comprising a fluoride source and a silica dental abrasive A dentifrice composition is described for combating dental erosion and/or tooth wear comprising a fluoride ion source and a silica dental abrasive, the dentifrice having a Relative Dentine Abrasivity (RDA) value from 20 to 60 and a pH in the range 6.5 to 7.5 and being free of an orthophosphate buffer or a water soluble salt of a C10-18 alkyl sulfate.
CN102805767A Heat stranguria removal granule raw material polygonum capitatum extract with anti-gonococcus effect The invention discloses a heat stranguria removal granule raw material polygonum capitatum extract with an anti-gonococcus effect, in particular to a polygonum capitatum extract. A preparation method of the polygonum capitatum extract comprises the following steps of: (1) adding 50-90 percent ethanol in an amount which is 5-15 times of the amount of fresh or dry product of the underground part of polygonum capitatum into the fresh or dry product of the underground part of polygonum capitatum to perform reflux extraction for one to three times, filtering, concentrating filtrate and drying to obtain alcoholic extract; (2) suspending the alcoholic extract in methanol, ultrasonically treating for 0.5-5 hours, centrifuging, and loading supernatant to an MCI macro-porous resin column; and (3) performing gradient elution by using water and 10-100 percent methanol in sequence, collecting each part of eluent, recovering solvent and drying a part obtained by elution of different solvents to obtain a methanol eluent or mixture thereof. The polygonum capitatum extract has the beneficial effects mentioned as the specification.
CN1827605A 4,4-disubstituted-3,4-dihydro-2(1H)- quinolones and synthesis process and use thereof The invention relates to a 4, 4-disubstitutional-3,4-dihydro-2(one hydro)-quinaldinicketones compound and its method for synthesizing and its application. The said compound can be a compound with its constitutional formula on tha right, or its stereoisomer, its stereoisomeric mixture or a salt which can be accepted in the pharmacy. The method for synthesizing chiral pure isomer is carried out mainly by the asymmetric additive reaction between substrates of methyl ketone and trifluoromethylketone imine. Additionally, we can construct the most critical trifluoromethyl quaternary carbon chiral center of the target compound DPC083 easily and efficiently. Afterwards, the synthesis of the target compound DPC083 is realized by the transformation of the function group.
US20100227002 Antioxidant compositions comprising extracts of myrtle and rosemary The invention relates to a composition based on extracts of myrtle and rosemary which has been found to synergistically increase the protection of cells against pathophysiological conditions characterised and partly caused by overproduction of free radicals and to counteract the oxidative stress caused by excessive production of said free radicals, as well as for preventing and/or treating related pathologies, including apoptosis.
US20060035923 Overactive bladder treating drug A therapeutic agent for overactive bladder containing tamsulosin or a pharmaceutically acceptable salt thereof as an effective ingredient.
CN101245035A Hydroxamic acid derivant, preparation method and antineoplastic application The invention relates to a compound in a formula (I); wherein, the enantiomer forms, the diastereoisomers, the racemates and the medicinal salts of each substituent group are defined by a specification; the invention also discloses a preparation method of the compound in the formula (I) and a drug composition comprising the compound, and the compound and the drug composition have antitumor activity.
WO2007043710A1 Novel dihydropseudoerythromycin derivatives Compounds represented by the general formula [I] (wherein each symbol is as defined in the description) or pharmacologically acceptable salts thereof; and pharmaceutical compositions containing the compounds or the salts as the active ingredient.
CN1969944A Oral compound western and Chinese integrated medicine for treating asthma and preparation process thereof The invention relates to a compound oral medicament for treating asthma and process for preparation, wherein the constituents include (by weight ratio) earthworm 15-20, licorice root 5-10, ammonium chloride 3-8, promethazine 0.2-0.5, gingko 6-9, Chinese ephedra 4-8, cerealose 10-15. The preparing process comprises the steps of disintegrating raw materials, mixing into tablets, powders and capsules.
CN103432143A Application of Chukrasone A in preparation of medicaments for treating blindgut cancer The invention discloses application of Chukrasone A in preparation of medicaments for treating blindgut cancer and belongs to the technical field of novel application of medicaments. An in-vitro MTT (methyl thiazolyl tetrazolium) anticancer activity evaluation discovers that Chukrasone A has a remarkable inhibition effect on the growth of human blindgut cancer cell strains HCT-8. Therefore, Chukrasone A can be used for preparing anti-blindgut cancer medicaments, and has an excellent development application prospect. The application of Chukrasone A in preparation of medicaments for treating blindgut cancer is disclosed for the first time, and the frame type belongs to a brand-new frame type, so that the inhibition activity of the Chukrasone A to blindgut cancer cells is unexpectedly strong.
CA2617979A1 Combination of a pyrimydlaminobenzamide tyrosine kinase inhibitor and a histone deacetylase inhibitor The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound; and b) an HDAC inhibitor compound. and a method for treating or preventing a proliferative disease using such a combination.
WO2013041810A9 Stable, low-toxicity, sterilizable composition for ophthalmic dying The invention relates to a stable composition for ophthalmic dying, suitable for sterilization in an autoclave, comprising the following in an aqueous solution: - at least a dye, - at least a water-soluble polyol with formula H(HCOH)nH, where n is a whole number greater than 3, for use in either of the two following methods: an ophthalmic surgical treatment method and a diagnosis method.
CN102827132A Alpha-mangostin amino-acid ester derivative, as well as preparation method and application thereof The invention relates to an alpha-mangostin amino-acid ester derivative in the structural formula (1), as well as a preparation method and application thereof. In the structure, R is various amino acids and hydrochlorides and acetates or other pharmaceutically acceptable salt groups thereof. The alpha-mangostin amino-acid ester derivative has antitumor activity, and can be used for preventing and treating cancers.
EP2117557A2 Compositions and methods for treatment of colorectal cancer We have identified a new variant of ileal bile acid binding protein (IBABP), designated IBABP-L, which is a biomarker for colorectal cancer. The transcript for IBABP-L arises from an alternative start site and includes three exons that are absent in IBABP. IBABP-L also shares part of a fourth exon with IBABP. The protein encoded by IBABP-L contains a deduced 49 residue N- terminal sequence that is not found in the IBABP protein. The present invention provides, for example, compositions and methods for diagnosing and treating colorectal cancer.
CN101584684A Enteric preparation containing stable salts of S-adenosyl-L-methionine and preparation method thereof The invention provides an enteric preparation including stable salts of S-adenosyl-L-methionine and the preparation method thereof. The enteric preparation is made by loading a plurality of independent enteric micropills including stable salts of S-adenosyl-L-methionine into a capsule, and characterized by no phenomenon of medicine burst release or local high concentration, not being affected by food, full medicine function, and slight untoward effect.
CN1843361A Cefditoren pivoxil dry suspensoid and its preparing process The invention relates to a Cefditoren pivoxil for suspension and its preparing process, wherein the preparation is prepared from Cefditoren pivoxil, cane sugar, methyl hydroxypropylcellulose, egg white sweets and orange essence through sieving, weighing, mixing homogeneously, charging adhesive, palletizing, forced air drying and granulating.
US20050063980 An alginate, a pectin and an antacid, such as sodium or potassium bicarbonate; gastrointestinal reflux disease The present invention relates to a gastric raft composition comprising alginic acid or a salt thereof, pectin and a gas producing material capable of producing a non-toxic gas when contacted with aqueous acid. The pectin is preferable a high ester pectin, such as methyl ester pectin and the alginic acid or the salt thereof is preferably of high guluronate content, such as for example sodium or potassium alginate. The gas producing material can be selected from sodium or potassium bicarbonate and the composition can further comprise a pharmaceutically acceptable ingredient, which is an antacid.
CN102206864A Agomelatine monocrystal with agomelatine VI crystal form, agomelatine mixed crystal with the agomelatine VI crystal form and preparation methods The invention discloses an agomelatine monocrystal with an agomelatine VI crystal form and a preparation method thereof, wherein the agomelatine VI crystal form is a novel crystal form of agomelatine. The invention also provides an agomelatine mixed crystal with the agomelatine VI crystal form and a preparation method thereof. The agomelatine mixed crystal has good effects of treating depression and anxiety. The invention further provided an application of the agomelatine mixed crystal with the agomelatine VI crystal form and an agomelatine II crystal form for preparations of medicines for treating cancers. The beneficial effects of the invention comprise providing an agomelatine monocrystal with agomelatine VI crystal form, an agomelatine mixed crystal with the agomelatine VI crystal form and an agomelatine II crystal form, and their preparation methods, wherein the agomelatine mixed crystal is superior to the agomelatine monocrystal in terms of dissolution rate and bioavailability. In addition, the agomelatine mixed crystal has a long-time stability and is suitable for storage without especial equipment, thus the agomelatine mixed crystal has an important superiority in a pharmacy industry.
CN101057842B Application of C60-benzoic acid nitrogen mustard in preparing medicine for anti tumor The invention discloses the use of nitrasin-based pharmaceutical C60-benzoic acid chlorethazine using C60 as the carrying agent in the preparation of anti-tumor agents, which has a structural formula I. It is found by the radioactive labeling technique employed in the invention that C60-benzoic acid chlorethazine has high assimilation ratio and longer detention time in stomach, and can improve the eradication action to the body tumor tissue, the tumor-resisting rate is higher than that of the chlorethazine for lymph metastasis.
US20110135571 Hybrid nanoparticles as anti-cancer therapeutic agents and dual therapeutic/imaging contrast agents The presently disclosed subject matter provides nanoscale coordination polymers for use as anticancer agents and as dual anticancer/imaging agents. The nanoscale coordination polymers can comprise a plurality of platinum metal complexes; nonplatinum anticancer drug bridging ligands complexed to multiple metal centers; or combinations thereof. The nanoscale coordination polymers can be targeted for delivery to cancer cells. They can also comprise stabilizing agents to allow for controlled and/or sustained release of anticancer agents in vivo.
US7678822 inhibiting rejection of a transplanted organ, tissue or cell in a recipient mammal; immunosuppressive agent; autoimmune diseases Methods of inducing immune tolerance by administering an immunosuppressive agent and a compound represented by Formula (I) are disclosed: Additionally methods of suppressing an immune response by administering an immunosuppressive agent and a compound represented by Formula (I) are disclosed. Further disclosed are methods for treating autoimmune diseases by administering an immunosuppressive agent and a compound represented by Formula (I). The variables of Formula (I) are described herein.
CN102675061A Ether derivative of resveratrol and medical application The invention provides an ether derivative of resveratrol and medical application, and belongs to the field of medicines. The compound with bioactivity is a compound of the general formula (I), salt, solvate or hydrate thereof, wherein X1 is H or CH2R1, X2 is H or CH2R2, X3 is H or CH2R3, but X1, X2 and X3 are not all H, and X1, X2 and X3 can be the same; R1, R2 and R3 are same or different, each of the R1, R2 and R3 is C1-6 alkyl substituted by R4, or 4-7 member ring which can be substituted by R9 arbitrarily and contains one or more additional heteroatom of O, S(O)n and NR9; R4 is F, CF3, OR5, NR6R7 or S(O)nR8; R5, R6 and R7 are same or different, each of the R5, R6 and R7 is C1-6 alkyl substituted by R4 arbitrarily, or NR6R7 is 4-6 heterocyclic alkyl ring containing heteroatoms of one or more O, NR9 and S(O)n; each n is 0-2; R8 is C1-6 alkyl; R9 is C1-4 alkyl defined by R4 or arbitrarily substituted by R4 or halogen; and R9 is H or C1-6 alkyl. The ether derivative can be applied to treatment of hepatic diseases, T-cell proliferation related or proinflammatory cytokine induced diseases.
CN1970556A 1-furfuryl-3-substituted Indolinyl-2-one derivative, its preparation method and uses The invention discloses a 1-(5-substituted furfuryl) indole-2-ketone compound of 3-aromatic methylene, C=N or C=O and analogue and making method and application on the medicine, which is characterized by the following: the compound possesses excellent antipiriculin activity in the test result; R1 is CHR4,NR5,O;R2 is H, halogen, hydrocarbon radical; R3 is O, indole ring, five-membered ring; R4 is aromatic radical, alkylene, substituted phenyl; R5 is -NHC (S) NH2.
CN103254212A Annonaceous acetogenins derivatives, and preparation method and purpose thereof The invention relates to annonaceous acetogenins derivatives, and a preparation method thereof and a purpose thereof in inhibiting tumors. The derivatives are characterized in that the structures of the derivatives are represented by a general formula (1). One or two groups of R1, R2 and R3, or one or two groups of R4, R2 and R3 are respectively hydroxyl; rest of the groups are biotin acyloxy, or 6-biotin acylamino hexanoyloxy, or 4-oxo-4-(6-biotin acylamino amine)butyryloxy; when R1 is the above group, R4 is H; and when R4 is the above group, R1 is H. 20 compounds are involved. According to the invention, through an esterification or acylation reaction, annonaceous acetogenins bullatacin or squamocin is directly coupled with biotin; or biotin is first connected with different linkers such that long-arm biotin is obtained, and the long-arm biotin is respectively coupled with bullatacin or squamocin; and separation purification is carried out through silica gel column chromatography and high-performance liquid-phase chromatography, such that the derivatives are obtained. The antitumor activity of the derivatives is higher than the parent compound bullatacin or squamocin.
WO2005080573A1 Recombinant viral vectors to promote neuronal cell survival and uses thereof The present invention relates to apoptosis. More specifically, the present invention is concerned with recombinant viral vectors to promote neural survival in glaucoma and other retinal diseases. A vector which expresses MEK nucleic acid sequence encoding a recombinant MEK product which is more active than a wild type MEK product, wherein said recombinant MEK is expressed to a level which is sufficient to enable an increase in activation of at least one of Erk1 and Erk2, thereby enabling neuronal survival of cells undergoing cell death is taught herein.
EP2029588A2 Tetrahydropyrido[3,4-d]pyrimidines and related analogues Tetrahydropyrido[3,4-d]pyrimidines and related analogues are provided, of the formula (I) in which variables are as described herein, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
WO2010028858A1 Use of cis-imidazolines, particularly nutlins, for treating chemo-resistant cancer diseases The present invention relates to a pharmaceutical composition, comprising cis-imidazoline inhibiting at least one or more ABC transporters, particularly nutlin, in combination with at least one or more cytostatic drugs, wherein the cytostatic drug may be transported out of a cancer cell by mediation of the ABC transporter, and to the use thereof for the treatment of cancer, and related aspects.
WO2006120412A1 Pharmaceutical formulation of apomorphine for buccal administration The present invention provides a kit comprising, in separate compartments of a container, the following components (a) and (b): (a) a combination of apomorphine or a pharmaceutically acceptable acid addition salt thereof and a pharmaceutically acceptable excipient or carrier; and (b) a solution which comprises a diluent and a pH modifying agent; the components being presented such that they can be combined at the point of use into a formulation which is adjusted to a pH ranging from mildly acidic to alkaline and which is suitable for buccal administration. The formulation is useful in treating Parkinson's disease and in promoting sexual function.
EP1303261B1 Self-emulsifying drug delivery systems for extremely water-insoluble, lipophilic drugs A formulation for administering an extremely water-insoluble active agent is disclosed. More particularly, a self-emulsifying drug delivery system for extremely water-insoluble, lipophilic compounds is disclosed.
US20110064828 Treatment of metastatic tumors and other conditions The present invention generally relates to pharmacology and, in particular, to the treatment of tumors and other conditions. In some aspects, the invention is directed to the treatment of subjects having tumors or cancers that are metastatic. Surprisingly, it has been found that certain compositions comprising oxidized glutathione-based compounds are able to effectively treat such cancers by inhibiting cell migration and/or invasion processes, and thus, inhibiting tumor cell metastases. Without being bound by any theory, it is believed that such compositions are effective since the compositions are able to suppress the activation of critical signaling pathways within cells that are used for cell migration, such as the ErbB2 and/or phosphoinositide-3 kinase (PI3K) pathways, including the downstream RhoA and AKT pathways. Such pathways are regulated by ERp5, which is a protein disulfide isomerase regulated using certain redox pathways, and those redox pathways are unusually sensitive to treatment using oxidized glutathione-based compounds. Thus, the composition of the instant invention, in some embodiments, are surprisingly effective at preventing tumor metastases. While other references have disclosed the treatment of cancers using oxidized glutathione-based compounds, no reference has suggested that signaling pathways used for cell migration, invasion and metastasis, such as the ErbB2, PI3K, RhoA, and AKT pathways, are highly susceptible to treatment by altering the redox state of the cell, e.g., by oxidized glutathione-based compounds. Accordingly, the use of such compositions to treat tumor metastases is surprising and could not be predicted given the teachings of the prior art.
US7307078 Polycyclic compounds which modulate PPARγ type receptors and cosmetic/pharmaceutical compositions comprised thereof Novel polycyclic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
US8026212 Methods of preparing pharmaceutical compositions comprising GPR119 agonists having the effect of glucose-dependent insulinotropic peptide secretatgogues The present invention relates to methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual. Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. Agonists of GPR119 receptor promote bone formation in an individual.
CA2496127C Piperidinyl compounds that selectively bind integrins The invention is directed to piperidinyl compounds of formula (I) and (II) that selectively bind integrin receptors and methods for treating an integrin mediated disorder, wherein W, R2, Z and q are described in the application.
CN203220605U Quick-acting tumor pain relieving bag The utility model relates to a quick-acting tumor pain relieving bag. The quick-acting tumor pain relieving bag mainly comprises an adhesive piece, a medical bag and an ointment. The quick-acting tumor pain relieving bag can be packaged into a vacuum-sealed thermal insulation bag, so that the ointment can be in a damp state all the time. The quick-acting tumor pain relieving bag has the advantages that a pain relieving effect is fast, the pain is immediately relieved after pain relieving cloth is applied to a painful part, completely disappears after 24-30 hours and cannot reappear; the quick-acting tumor pain relieving bag is mainly used for relieving the pains of tumor patients, and particularly early cancer patients.
US7390905 Tachykinin receptor antagonists for use treating e.g. emesis, depression, urinary disorder The present invention relates to a piperidine compound represented by the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted benzene ring, R1 represents an optionally substituted hydoxyl group, a substituted thiol group, a substituted sulfonyl group, etc., or a group represented by the formula: R11 represents a substituted carbonyl group or a substituted sulfonyl group, R12 represents hydrogen atom or an optionally substituted alkyl group, R2 represents hydrogen atom, etc., Z represent oxygen atom or a group represented by —N(R3)—, R3 represents an optionally substituted alkyl group, etc., R4a represents an optionally substituted alkyl group, R4b represents an optionally substituted alkyl group, or a pharmaceutically acceptable salt thereof, having an excellent tachykinin receptor antagonistic action.
US20120059023 Use of polymorphic forms of rifaximin for medical preparations The present invention relates to Rifaximin polymorphic forms α, β and γ, to their use in medicinal preparations for the oral or topical route and to therapeutic methods using them.
WO2009131065A1 Long-chain fatty acid elongation enzyme inhibitor comprising arylsulfonyl derivative as active ingredient Disclosed is a compound useful as a prophylactic agent or a therapeutic agent for cardiovascular diseases, nervous system diseases, metabolic diseases, genital diseases, gastrointestinal diseases, neoplasm, infectious diseases and others or an herbicide. Specifically disclosed is a long-chain fatty acid elongation enzyme inhibitor comprising a compound represented by formula (I) [wherein W represents a hydrogen atom, a C1-6 alkyl or the like; X represents an aryl, a heteroaryl or the like; n represents a number of 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl or the like; and A1, A2, A3 and A4 independently represent CH or N] or a pharmaceutically acceptable salt thereof as an active ingredient.
WO2012020836A1 Therapeutic agent for hepatitis c containing rrm2 antagonist as active ingredient The present invention addresses the problem of providing a therapeutic agent for hepatitis C containing an RRM2 antagonist as the active ingredient, an oligoribonucleotide for suppressing the expression of RRM2, a vector for expressing the oligoribonucleotide, and a method for inhibiting the expression of RRM2 by combining the oligoribonucleotide with RRM2 RNA. In order to solve the problem, the present inventors first identified the siRNA sequence that binds to the IRES region of HCV and that exhibits RNAi activity against the ribonucleotide reductase M2 subunit that has been recognized as having an important role in HCV replication, and then reverse transfected the siRNA molecules into persistently HCV-infected cells and measured replicon cytotoxicity. As a result, the siRNA molecules of the present invention were found to exhibit significant HCV replication-suppressing activity.
CN101972265A Medicament for treating impotence The invention relates to a medicament for treating impotence, which is prepared by mixing the following medicaments in part by weight: 0.5 to 3 parts of dexamethasone and 10 to 100 parts of aspirin. The medicament is used for treating pathological impotence and ensures the cure rate of over 80 percent.
WO2007065662A3 Trisubstituted quinazolinone derivatives as vanilloid antagonists The present invention relates to quinazolinone compounds of the formula wherein R2, R3, R5, R6 R7 and R8 are as defined in the specification and in the claims, in free form or in salt form, processes for their preparation and their use as pharmaceuticals, particularly in the treatment of disorders ameliorated by administration of TRPV1 antagonists.
US20100323998 Topical composition containing the combination of mupirocin and beclomethasone The present invention relates to a topical pharmaceutical composition comprising mupirocin and beclomethasone, a process for its preparation, its use in the treatment of infected dermatoses caused by bacteria susceptible to mupirocin and in the treatment of secondary bacterial infections in patients of steroid responsive dermatoses.
WO2007084314A3 MODULATORS OF 11-ß HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 such as obesity and diabetes.
CN103463052A Application of Lycojaponicumin A in drugs for treating cervical cancer The invention discloses application of Lycojaponicumin A in preparation of drugs for treating cervical cancer and belongs to the technical field of new application of drugs. In vitro MTT anticancer activity evaluation discovers that Lycojaponicumin A shows remarkable inhibitory effects on growth of human cervical carcinoma cell lines HeLG, HeLG229, HCE1 and CaSKi. Therefore, the Lycojaponicumin A can be used for preparing anti-cervical cancer drugs and has good development and application prospects. Application of the Lycojaponicumin A in preparation of drugs for treating cervical cancer is disclosed for the first time; and because skeleton type is completely new, inhibitory activity on human cervical cancer cells is extraordinary strong.
EP1685115A1 Novel norepinephrine reuptake inhibitors for the treatment of central nervous system disorders This invention relates to compounds of the formula (I), wherein R1, R2, and R3 and R4 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.
US20110301452 Microcapsule for local treatment of a tumor and method for positioning a magnetic gradient field guiding magnetic nanoparticles to a target location as well as apparatus for positioning a magnetic gradient field A microcapsule for the local treatment of a tumor is proposed. The microcapsule has a support material forming a casing for the microcapsule, an active agent that damages tumor cells, a marker material suitable for use as an x-ray marker, and at least one magnetic nanoparticle. The active agent in particular destroys the tumor cells.
WO2009151613A1 Oxybutynin derivatives This invention relates to novel compounds that are phenylglycolic acid derivatives, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel phenylglycolic acid compounds that are derivatives of the muscarinic acetylcholine receptor antagonist, oxybutynin. This invention also provides pyrogen-free pharmaceutical compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering muscarinic acetylcholine receptor antagonists. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving oxybutynin.
WO2009104990A1 2,4-diaminopyridine derivatives, a pharmaceutical composition and a medicinal agent which are based thereon and used for treating or preventing diseases and disturbances caused by the hyperactivation of nmda-receptors and/or in the form of cognitive function stimulators and a method for the use thereof The invention relates to novel 2,4-diaminopyridine derivatives, pharmaceutically acceptable salts and /or solvates thereof, to compositions and medicinal agents containing the novel 2,4-diaminopyridine derivatives and to the use thereof as the NMDA-receptor blockers and cognitive function stimulators. The novel derivatives combine the properties of highly affine NMDA-receptor antagonist with the properties of moderate acetylcholinesterase inhibitors and with the properties of highly affine agonists of nicotine cholinoreceptors and sympathomimetics, whereby determining the comprehensive normalising action thereof on the disballance of several neurotransmitting systems, including glytamatergic, cholinergic and adrenergic systems without undesirable side effects which were previously observed in the known NMDA-antagonists. They not only do not cause the disturbance of intellectual abilities, attention and memory that is typical for the known NMDA-receptor antagonists, but, in addition, can be useful for treating and preventing a range of diseases and disturbances related to disturbed cognitive functions and learning ability. The method for treating or preventing diseases and disorders caused by the incresed activation of the glutamatergic system and/or by the damage of intellectual mnestic functions.
CN102068412A Enteric targeted tilmicosin particles and preparation method thereof The invention discloses enteric targeted tilmicosin particles and a preparation method thereof, which relate to the enteric targeted particles and the preparation method thereof and aim to solve the problems of difficulties in administration in an administration process. The enteric targeted tilmicosin particles consist of tilmicosin, a bonding agent and a coating fluid. The preparation method for the enteric targeted tilmicosin particles is implemented by the following steps of: 1, preparing the bonding agent; 2, preparing particles; 3, preparing the coating fluid; 4, coating the particles; and 5, drying the particles. In the invention, enteric coating technology is adopted, the tilmicosin is prepared into the enteric targeted particles, and the intrinsic bitterness and irritation of the medicaments are hidden, thereby solving the problems of difficulties in the administration. The preparation method is particularly applied in the field of preparation of the enteric targeted particles.
CN101002941A Anticarcinogen composition carried with platinum compound and vasoinhibitor An anticancer composite medicine in the form of slowly-released injection or slowly-released implant is composed of the slowly-released microballs consisting of vascular depressant (sirolimus, tacrolimus, etc) and slow-releasing assistant, and the special solvent containing suspending aid.
CN1813687A Method for preparing tinidazole biological composite membrane The present invention relates to a preparation method of tinidazole biological complex membrane. Said preparation method includes the following steps: slowly adding 0.05-2.0% of sodium alginate solution into mixed aqueous solution of 0.01-2.0% of chitosan solution and 0.05-0.5% of tinidazole solution, the pH value of the described chitosan solution is 4-6, under the condition of stirring according to 150-5000 rpm making reaction for 30-60 min to obtain sodium alginate-chitosan gel beads, making centrifugal treatment, adding calcium chloride aqueous solution, stirring with 5000-10000 rpm and making reaction for 30-120 min, pouring the obtained mixed suspension into culture dish, drying in drying oven so as to obtain the invented tinidazole biological complex membrane.
CN101385710A Anticancer composition loaded with cyclophosphamide and carmustine An anticancer composition carrying cyclophosphamide and carmustine is a sustained release injection which consists of sustained release microspheres and a dissolvent, wherein, the sustained release microspheres comprise an anticancer active component and a sustained release adjuvant, and the dissolvent is a common dissolvent or a special dissolvent containing a suspending agent. The suspending agent has the viscosity of 100cp-3000cp (at the temperature of 20-30 DEG C) and is selected from sodium carboxymethyl cellulose and the like; the anticancer active component is a combination of a nitrosourea drug and an alkylating agent selected from the melphalan, ifosfamide, 4H-peroxy-cyclophosphamide or norcantharidin; the sustained release adjuvant is selected from copolymer of polyphosphate esters such as p(LAEG-EOP), p(DAPG-EOP) and the like, copolymer of the polyphosphate esters and polylactic acid, polifeprosan, dienoic fatty acid and sebacic acid, or copolymer or polyblend of poly(erucic acid dimmer-sebacic acid) or poly(fumaric acid-sebacic acid); the anticancer composition is also made into a sustained release implant, and injected into or placed inside or at the periphery of tumor to keep the effective drug concentration more than 60 days. The anticancer composition can also obviously reduce the general reaction of the drug, and selectively enhance the curative effects of non-operative therapies such as radiotherapy, chemotherapy and the like.
CN101427995A Anticancer sustained-release agent The invention relates to sustained-release injection for cancer therapy. The sustained-release injection comprises sustained-release microspheres and dissolvent, wherein the sustained-release microspheres comprise active ingredients for cancer therapy and sustained-release auxiliary materials, and the dissolvent is special dissolvent containing suspending agent. The active ingredients for cancer therapy comprise bendamustine and cytotoxic drug; the cytotoxic drug is selected from taxane, alkylating agent, topoisomerase inhibitor and/or plant alkaloid; the sustained-release auxiliary materials comprise polylactic acid and the glycolic copolymer thereof, polyethylene glycol and the polylactic copolymer thereof, terminal carboxyl polylactic copolymer, EVAc, fatty acid and decanedioic copolymer; the viscocity of the suspending agent is 100cp to 3000cp (at 25 to 30 DEG C), and the suspending agent is selected from sodium carboxymethyl cellulose. The sustained-release microspheres can also be produced into sustained-release implant, and by injecting or positioning the preparation or sustained-release implant in tumor or tumor margin, the general reaction of the drug can be reduced and simultaneously the local concentration can be selectively improved and maintained for approximately 30 to 50 days; therefore, besides being independently applied for oncotherapy, the sustained-release injection for cancer therapy can also enhance the tumor inhibition effect of non-operative treatment such as chemical treatment and/or radiation treatment.
WO2005025520A3 Chitosan spinning method, device therefor, and resulting chitosan yarn, and uses thereof The invention concerns a chitosan spinning method characterized in that it consists in subjecting the chitosan collodion to the coagulating action of a gas, preferably ammonia. The invention also concerns a device for implementing said method, which consists in placing the extrusion die output in a coagulating gas atmosphere. The invention further concerns the yarn obtained by said method and uses thereof in various types of industries.
WO2010027189A9 A new use for homoisoflavanone or a salt thereof The present invention relates to a new use for homoisoflavanone or a salt thereof. More particularly, it relates to a pharmaceutical composition for the prevention and treatment of inflammatory disease or allergy comprising homoisoflavanone or a salt thereof according to chemical formula 1; the use of homoisoflavanone or a salt thereof in the manufacture of a drug for the prevention and treatment of inflammatory disease or allergy; and a method for the treatment of inflammatory disease or allergy characterised by administering to an individual the required dose of homoisoflavanone or a salt thereof as the active ingredient.
CN102557893A Lignan compounds with glucokinase (GK) activation effect The invention relates to a series of lignan compounds which are tatarinan A-R extracted and separated from glassleaved sweetflag rhizome, pharmaceutical compositions of the lignan compounds and application of the lignan compounds.
US7232816 Phosphodiesterase inhibitors; used to treat inflammatory conditions, allergies such as rhinitis, respiratory system disorders and cancer The invention relates to novel substituted pyrazolo[4,3-e]-diazepines of general formula: to pharmaceutical compositions containing them, to their use as medicinal products and to processes for preparing them.
CN1857221A Slow released anticancer medicien containing both platinum compound and its synergist The slow released injection containing both platinum compound and its synergist consists of slow released microsphere and solvent. The solvent is special solvent containing suspending agent, and the suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The effective anticancer component is platinum compound dicycloplatin, etc or the composition of platinum compound and platinum compound synergist selected from antimitotic medicine and alkylating agent. The slow releasing supplementary material is selected from difatty acid-sebacic acid copolymer, poly (erucic acid dipolymer-sebacic acid), poly (fumaric acid-sebacic acid), etc. The slow released microsphere may be also prepared into slow released implanting agent set or injected to in tumor to lower the systemic toxic reaction, raise the local tumor medicine concentration and to raise chemotherapeutic and radiotherapeutic effect.
CN101766692A Channel-freeing harmonizing emulsion The invention provides a channel-freeing harmonizing emulsion for relaxing tendons and collaterals, expelling wind and dissipating blood stasis. The components of the emulsion are proportioned in mass percent as follows: 12-17 percent of olibanum oil, 15-22 percnet of methyl salicylate, 16-22 percent of pennyroyal, 8-12 percent of shortstalk monkshood root oil, 3-6 percent of myrrh oil, 3-6 percent of azone, 5-10 percent of stearic acid, 3-6 percent of castor oil, 5-10 percent of eucalyptus oil and 5-10 percent of white oil. The channel-freeing harmonizing emulsion can dredge the points and the channels at the focal locations; eliminate stasis in channels according to the conduction function of channels to strengthening qi and blood, dispel cold in blood, disperse stasis in blood and promote blood circulation; expel symptoms of wind, cold, moisture, heat and toxin in the human body; relax tendons and collaterals, promote blood circulation by removing blood stasis, dispel wind and moisture and release swelling analgesia; and realize the purposes of curing internal disease by external curative and treating both principal and secondary aspects of disease.
EP2376428A2 New inhibitors for treating diseases associated with an excess transport of hyaluronan The present invention relates in general to a compound which is characterized by a formula selected from the following formulas A, B, C, D, E or F; or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the inhibitor(s) of the invention and to their use in the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention furthermore relates to the use of at least one inhibitor of the invention for the preparation of a pharmaceutical composition for the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the inhibitor defined herein in a pharmaceutically acceptable form.
CN100999471A Production tech. of acid type lovastatin and production tech of its salt and pharmaceutical application A lovastatin acid and lovastatin acid salt production processes and their application, to solve the problem of significantly toxicity of lactone form lovastatin, such as liver injury and causing muscle pain and elevating transaminase. The invention uses 95% ethanol and NaOH (13 ~ 100:8 that m lactone structure: mNaOH) to modulate into alkaline solution, makes lactone lovastatin powder dissolved in solution, and uses HCl adjust PH to obtain the acid form and salt state compounds, widely used for lipid drug.
CN102796118A Cefodizime sodium compound solid, method for preparing same and pharmaceutical preparation of cefodizime sodium compound solid The invention discloses a cefodizime sodium compound solid, a method for preparing the same and a pharmaceutical preparation of the cefodizime sodium compound solid, wherein the method for preparing the cefodizime sodium compound solid comprises the following steps of: first, dissolving crude cefodizime sodium salt in an acetone aqueous solution, then adding activated carbon to adsorb and filter, cooling the filtrate, stirring to separate the solid out, adding an acetone solvent to separate the solid out, filtering and drying, thus obtaining the cefodizime sodium compound solid. The prepared compound solids are fine particles, and have uniform particle size distribution and good liquidity, the crystallization technology is simple, the residual amount of organic solvent is low, and the product stability and pharmaceutical safety are effectively improved.
US20130012524 Stabilized prolonged release pharmaceutical composition comprising atypical antipsychotic The present invention provides stabilized prolonged release pharmaceutical compositions comprising atypical antipsychotic drug like paliperidone or pharmaceutically acceptable salts thereof without incorporating surfactant and/or water penetration enhancer. Such compositions are preferably in the form of a matrix wherein one or more release controlling agents are present in and/or on the matrix. Further, such compositions comprise one or more release controlling agent and exhibits desired in vitro release of drug with or without lag period. The invention also provides a process for the preparation of such compositions.
WO2007132714A1 Agent for increasing bone density It is intended to provide an agent for increasing bone density which can increase bone density and thus exerts preventive and therapeutic effects on diseases relating to bone such as osteoporosis, osteoporosis caused by menopause or hyperparathyroidism, secondary osteoporosis or retarded osteogenesis caused by gonadal dysfunction, more specifically speaking, an agent for increasing bone density which comprises as the active ingredient a medium chain fatty acid and/or an acyl glycerol containing a medium chain fatty acid. It is also intended to provide a food, a drink, a drug or the like which has an effect of increasing bone density and is useful in preventing and treating osteoporosis, bone fracture and so on. An agent for increasing bone density which comprises as the active ingredient a medium chain fatty acid and/or an acyl glycerol containing a medium chain fatty acid. A food or a drink which contains this agent for increasing bone density and is useful in preventing or treating osteoporosis.
CN102552252A Medicine preparation of temozolomide and preparation method thereof The invention discloses a medicine preparation of temozolomide, which comprises the following ingredients: 5-20% of temozolomide, 5-30% of solubilizer, 30-50% of cryoprotectant, 5-20% of first buffering agent, 5-15% of second buffering agent. In the preparation, firstly, the temozolomide raw material is subjected to ultramicro smashing by airflow to about 1-10 micrometers, and the solubilizer only adopts polyethylene glycol-15-hydroxyl stearate. According to the preparation disclosed by the invention, solution preparation time is greatly shortened, and anaphylactic reaction and hemolysis caused by Tween-80 can be eliminated. The medicine preparation of the temozolomide has the advantages of simple formula composition, simple and convenient preparation technology, controllable quality and low cost and is suitable for industrial production.
WO2014060398A1 Ethynyl derivatives as modulators of mglur5 receptor activity The present invention relates to ethynyl derivatives of formula (I) wherein Y is N or CH R1 is fluoro or chloro R2 is hydrogen or methyl or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
EP2731948A1 Novel substituted indole derivatives as gamma secretase modulators The present invention is concerned with novel substituted indole derivatives of Formula (I) wherein R1, R2, R3, A1, A2, A3, Y and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
CN102327268A Oral liquid for treating coccidium and white diarrhea polyinfection and preparation method thereof The invention discloses an oral liquid for treating coccidium and white diarrhea polyinfection and a preparation method thereof, and aims at providing the oral liquid, which is easy to use, for treating the coccidium and white diarrhea polyinfection effectively and efficiently and the preparation method with a simple process and easiness in realization. Every 100L of the oral liquid comprises 0.2-0.8kg of diclazuril, 5-15kg of propacin, 50kg of dimethylformamide, 0.4-1.6kg of neovaricaine and the balance of 95 percent ethanol. The diclazuril adopted by the invention is a broad spectrum anticoccidiosis medicament and is effective for tender coccidian, stack coccidian and the like; the propacin can be used for effectively resisting salmonella and killing pathogeny causing the white diarrhea; and the polyinfection is pointedly treated by combining the diclazuril with the propacin. According to the method disclosed by the invention, the propacin and the diclazuril are prepared into the solution which is enabled to be dissolved in water; and the coccidium and white diarrhea polyinfection is pointedly treated by drinking water and administrating, thus a better effect is obtained and the economic loss of raisers is avoided.
EP2759297A1 Combination therapy using p53 activator and c-Met inhibitor A pharmaceutical composition comprising a p53 activator and a c-Met inhibitor for use in combination therapy of preventing or treating a cancer is provided.
CN102838685A Wintergreen pure polysaccharide LTC-0-1 and application thereof The invention provides a wintergreen pure polysaccharide LTC-0-1 and an application thereof, which belong to the field of medicines and healthcare foods. The invention discloses an extracting method of the wintergreen pure polysaccharide LTC-0-1, a composition of the LTC-0-1 and a molecular weight of the LTC-0-1; it is proved by experiments that the LTC-0-1 can be used for increasing average lengths of hippocampal neurons of a GFP green fluorescent protein transgenic mouse, increasing the number of the neurons, obviously increasing dendritic spine densities of neuron dendrons in a unit length, increasing neuronal post-synaptic membrane protein expression and promoting the neurons to be more mature; the LTC-0-1 can be also used for inducing neuron-like differentiation of PC12 cells, promoting enation of the cells, enhancing activity of cell acetylcholinesterase AchE and increasing expression index of cell growth related protein GAP-43 and obtains neurotrophic activity; and the LTC-0-1 shows a growth promoting effect, a differentiation effect, a maturing effect and a damaged nerve cell function recovery effect on nerve cells and has broad prospects in development and application in the technical field of medicines and healthcare foods.
WO2013005798A1 Novel nitrogenated heterocyclic ring derivative A PDE10 inhibitor having excellent effectiveness, particularly a prophylactic or therapeutic agent for mental diseases such as schizophrenia and the like, has been demanded. The present invention provides: a nitrogenated heterocyclic ring compound represented by formula (I), a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt; and a pharmaceutical composition characterized by containing the compound, a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt as an active ingredient. The pharmaceutical composition is particularly a PDE10 inhibitor and can be used as a prophylactic or therapeutic agent for mental diseases such as schizophrenia and the like.
CN102442931A Methionine-deviated peptide mimics and use in protection for mitochondrions of skin cells The present invention relates to methionine-deviated peptide mimics and use in protection for mitochondrions of skin cells. The invention relates to a group of peptide mimics which are selected and are deviated from methionine amino acid, and to the use of the peptide mimics as protection agents for the mitochondrions of the skin cells. The invention also relates to a cosmetic composition or dermatopathology composition for preventing and treating skin diseases which are related with mitochondrion dysfunction.
US8057825 Krill extracts for treatment of cardiovascular diseases The present invention relates to a method of treatment and/or prevention of cardiovascular disease, rheumatoid arthritis, skin cancer, premenstrual syndrome, diabetes and transdermal transport enhancement. The method comprises the administration of a therapeutically effective amount of krill and/or marine oil to a patient. The present invention also relates to a composition for the treatment and/or prevention of these diseases.
US20080200470 serotonin 5-HT1A receptor agonists; N-heterocyclclediones substituted with a chroman-2-yl, 2-quinolyl, or phenoxy group; 2-[4-[(Chroman-2-yl)methylamino]butyl]-1,3-dioxoperhydroimidazo[1,5-a]pyridine; Parkinson's, cerebral damage by thromboembolitic ictus, depression, migraine, psychosis, urinary disorde The present invention relates to certain derivatives of cycloalkanediones invariably substituted with a chroman-2-yl, 2-quinolyl or —O-phenyl residue which are serotonin (5-hydroxytryptamine, 5-HT) 5-HT1A receptor subtype agonists modulators, to their stereochemical isomers and to their use in the preparation of a medicament for the treatment of pathological states for which an agonist a modulator of these receptors is indicated.
CN1799549A Process for preparing soybean isoflavone phospholipid composition The invention provides a process for preparing soybean isoflavones and phosphatide compound, which consists of dissolving phosphatides into water by the proportion of 1 : 20-500, dissolving soybean isoflavones into ethanol, mixing the two solutions into clarifying solvent, finally subjecting the filter liquor to decompression drying or freeze drying.
WO2014090306A1 Artemisinin and its derivatives for use in the treatment of kidney disease The present invention relates compounds according to Formula (I) wherein R1 and R2 are independently H or an optionally substituted group selected from an alkyl, a heteroalkyl, an aryl, a heteroaryl, an arylalkyl, and a heteroarylalkyl, and R3 and R4 taken together form a carbonyl (=O); or wherein R1 and R2 are independently H or an optionally substituted group selected from an alkyl, a heteroalkyl, an aryl, a heteroaryl, an arylalkyl, and a heteroarylalkyl, R3 is H and R4 is H or -OR5, wherein R5 is H or an optionally substituted group selected from an alkyl, a heteroalkyl, an aryl, a heteroaryl, an arylalkyl, and a heteroarylalkyl; or pharmaceutically acceptable salts or esters thereof, for use in the treatment of kidney disease, in particular in the treatment of acute kidney injury. The present invention also relates to methods of treatment of the same and methods of kidney transplant surgery and coronary artery bypass graft surgery using the compounds of Formula (I).
CN101496811A Soluble and stable tilmicosin composition The invention relates to a soluble and stable Tilmicosin composition. The soluble preparation consists of the following components: Tilmicosin, a latent solvent, a pH value stabilizing agent and proper auxiliary materials. The Tilmicosin obtained by the invention can be quickly dissolved into water and the effective components cannot be degraded with the prolonging of the placing time of an aqueous solution. The preparation composition can be combined with other substances for use so as to strengthen the drug effect. The composition is mainly used for treating respiratory tract infection, mixed infection of mycoplasma and Escherichia coli, other various pneumonia and pulmonary infectious diseases of livestock and poultry caused by Pasteurella, the mycoplasma, and the like.
US20060099158 Preparation containing conjugated linoleic alcohol Compositions comprising at least one conjugated linoleyl alcohol component selected from the group consisting of cis- and trans-isomers of 6,8-octadecadienol, 7,9-octadecadienol, 8,10-octadecadienol, 9, 11-octadecadienol, 10,12-octadecadienol and 11,13-octadecadienol are described along with their use in oral and topical applications for humans and animals.
CN103739615A Ketone compound with antitumor activity and application of ketone compound The invention belongs to the technical field of medicines and particularly relates to a ketone compound with antitumor activity and an application of the ketone compound. The invention discloses the ketone compound as shown in the general formula (I), an isomer of the compound as shown in the general formula (I) and a salt of the compound as shown in the general formula (I), wherein R1, R2 and R3 can be same or different and are all selected from hydrogen, halogen, a cyano group, a halogenated alkyl group, an alkoxy group, an alkoxyalkyl group, an alkylamino group or an alkylaminoalkyl group, and X is an oxygen, sulfur, carbon or nitrogen atom. A pharmacological activity screening result proves that the compound provided by the invention has a favorable inhibiting effect on MCF-7 (human breast cancer cells), HeLa (human cervical cancer cells) and Bel7402 (human hepatoma cells) and has favorable development and application prospects in the anti-cancer aspect.
US20110033469 Leukotriene b4 binding soluble lipocalin receptor from ixodes ricinus Leukotriene B4 binding polypeptide is obtained from Ixodes ricinus, the polynucleotide and related polypeptides may be used as research reagents and materials for the development of treatments and diagnostics tools specific to animal and human diseases.
CN103040836A Use of moclobemide in prostatic cancer resistance and pharmaceutical preparation of moclobemide The invention relates to the use of moclobemide and a pharmaceutical preparation of the moclobemide, and in particular relates to the application of moclobemide in preparation of a medicine for treating prostatic cancer. The invention further discloses clinically acceptable pharmaceutical preparations, such as tablets, capsules, pills which are prepared by taking the moclobemide as a medicine preparation raw material. The moclobemide and the pharmaceutical preparation of the moclobemide provided by the invention are very good in the action of prostatic cancer resistance, so that the moclobemide and the pharmaceutical preparation of the moclobemide are obvious in antitumor activity for the transplanted tumor in nude mice of the androgen-dependent and androgen-independent human prostatic cancer cell. Furthermore, the moclobemide is used in clinic as an antidepressant medicine, so that the moclobemide has the clinically-proved advantage of small toxic and side effects relative to the other anti-prostatic cancer chemotherapeutic medicines.
US20080213393 Solid dosage forms; using polyoxyethylene glycol binder; antacids; antidepressants; blood pressure medications; calcium channel blockers; calcium supplements; chemotherapy medications; cold medicines; antihistamines; maintaining or promoting the elimination of feces in the bowel This invention relates to novel colonic purgative compositions in a solid dosage form, comprising at least one purgative and at least one soluble, or soluble, nonfermentable binder, such as polyethylene glycol. Further, this invention relates to methods of using the colonic purgative compositions. The present compositions and methods are designed to improve patient tolerance and compliance, while at the same time improving the quality of bowel cleansing. The formulations and methods of this invention are particularly useful to cleanse the bowel prior to diagnostic and surgical procedures and can also be employed in lower dosages as a laxative to promote elimination and/or to relieve constipation.
US20110182970 Nitric oxide sensors and systems The present disclosure relates to nitric oxide sensors and systems.
WO2009022633A1 Bicyclic acylguanidine derivative Disclosed is a novel and excellent therapeutic or prophylactic agent for dementia, schizophrenia or the like, which relies on its serotonin 5-HT5A receptor modulation activity. Disclosed is a bicyclic acylguanidine derivative characterized by having such a structure that guanidine is bound to one ring in a bicyclic structure (e.g., chromene, dihydronaphthalene) via a carbonyl group and a cyclic group is bound to the other ring in the bicyclic structure. It is confirmed that the derivative has a potent 5-HT5A receptor modulation activity and an excellent pharmacological activity relying on the 5-HT5A receptor modulation activity. The derivative is useful as a good therapeutic or prophylactic agent for dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
US7112603 Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
WO2010074219A1 Benzothiophen compound Disclosed is a compound useful as an active ingredient of a pharmaceutical composition for treating diabetes. Extensive studies have been made on compounds having an SGLT-1/SGLT-2 dual inhibitory activity, and it is found that a benzothiophen compound of the invention has an SGLT-1/SGLT-2 dual inhibitory activity, exhibits an excellent hypoglycemic activity on a mild hyperglycemic condition as well as a severe hyperglycemic condition and therefore has an excellent hypoglycemic activity regardless of the severity of the hyperglycemic condition, and also has an excellent urinary glucose excretion activity on a condition having a normal blood glucose level. It is also found that the benzothiophen compound has an extremely high hypoglycemic activity on a mild hyperglycemic condition compared to those of compounds that can inhibit SGLT-2 selectively. The compound has an SGLT-1/SGLT-2 dual inhibitory activity, an excellent hypoglycemic activity regardless of the severity of the hyperglycemic condition and an excellent urinary glucose excretion activity on a condition having a normal blood glucose level, and therefore can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating diabetes-related diseases including type-1 diabetes, type-2 diabetes, insulin resistance disease and obesity and fatty liver diseases including nonalcoholic steatohepatitis (NASH).
WO2014026582A1 Tenofovir diester compound, preparation method and use thereof, and pharmaceutical composition comprising the same Disclosed is a Tenofovir diester compound shown as a general formula (I), a salt or tautomer thereof，as well as a preparation method and use thereof and a pharmaceutical composition comprising the same. The compound has good liposolubility, and strong anti-HIV effect and anti-HBV effect.
EP1185493B1 Quinones for treatment of diseases Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.
US20080214528 e.g. N-[3-{1-[(cyclobutyl)amino]-4-hydroxy-2-oxo-1,2-dihydro-quinolin -3-yl}-1,1-dioxo-1,4-dihydro-1 lambda 6-thieno[2,3-e][1,2,4]thiadiazin-7-yl)methyl]methane-sulfonamide; viricides for infections caused by an RNA-containing virus; hepatitis C virus (HCV) polymerase inhibitor; liver cirrhosis The present invention provides HCV polymerase inhibiting compounds having the formula (I): where R1 is cyclobutyl—N(Ra)-, n is 1, 2, 3 or 4, and at least one R5 is RaSO2N(Rj)alkyl-, In a non-limiting example, a compound of the present invention is N-[(3-{1-[(cyclobutyl)amino])-4-hydroxy -2-oxo-1,2-dihydro-quinolin-3-yl}-1,1-dioxo-1,4-dihydro-1λ6-thieno[2,3-e][1,2,4]thiadiazin-7-yl)methyl]methane-sulfonamide. The present invention also features compositions comprising the compounds of the present invention or pharmaceutically acceptable salts, stereoisomers or tautomers thereof, and methods of using the same to treat or prevent HCV infection.
CN1569009A Dripping pills of acetylgastrodin for treating nervous headache and its preparing method The invention provides dripping pills of acetylgastrodin for treating nervous headache and its preparing method, wherein the dripping pills are prepared form acetylgastrodin and dripping pill base material through stirring homogeneously, heating till melting, placing into dripping pills machine, instilling into condensation agent, forming ball-shaped bolus, and removing the condensation agent.
CN103417532A Sesquiterpene lactone compound and uses of derivative thereof in preparation of drugs The invention relates to a sesquiterpene lactone compound and uses of a derivative thereof in preparation of drugs, belongs to the technical field of the drugs, specially relates to the uses of a formula (I) compound in preparation of the drugs, and particularly relates to the uses of a formula (I) compound in preparation of the drugs for treatment of rheumatoid arthritis and treatment of cancer through inhibition of cancer stem cells.
WO2013020930A1 Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy The present invention relates to aminochromane, aminothiochromane and 1,2,3,4-tetrahydroquinoline derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino- 1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
CN101040712A Compound containing DAG and the method for preparing the same The invention provides a method for preparing a compound with diacylglyceride, via enzyme catalysis. The inventive compound comprises aliphatic acid glyceride as main component, wherein the diacylglyceride comprises 20-50% diacylglyceride, 20-40% oleic acid acyl-linolic acid acyl glycerin, 15-40% 2-oleic acid acyl glycerin, 3-10% linolenic acid acyl-linolic acid acyl glycerin, and 0-3% 2-glyceryl palmitate. And the content of diacylglyceride of inventive product is higher than 94%, with high unsaturated degree of fatty acid, lower than 3% of 2-santuraed acyl glycerin, and lower than 5% 3-acyl glycerin, while the compound is clear and transparent at normal temperature or lower temperature. And the invention uses 1-acyl glycerin as material with low cost, wide resource and low producing lost.
EP1556057A2 Agents and methods for enhancing bone formation The present invention discloses agents and methods for inducing osteoblastic cellular differentiation, as well as the use of such agents and methods to treat patients to maintain bone mass, enhance bone formation and/or bone repair. Exemplary agents include oxysterols, alone or in combination with particular oxysterols, or other agents known to assist in bone formation. The invention further includes medicaments including oxysterols for the treatment of bone disorders, local injections of oxysterols or cells (206) and implants (202) having agents or cells (203) to facilitate bone repair.
CN101385716A Sitafloxacin hydrate granules and preparation method thereof The invention relates to sitafloxacin particles and a production method thereof, each bag contains 25-200mg of sitafloxacin and pharmaceutical excipients, the pharmaceutical excipients mainly comprise 9 parts of lactose, 10 parts of soluble starch and lubricant; the preparation method is as follows: the sitafloxacin and the lactose are evenly mixed and then granulated, the lubricant is added after the granulation, and the filling is carried out, thereby preparing the sitafloxacin particles. The product has the advantages of stable quality, convenient carry and drug delivery and fast dissolution of active ingredients.
WO2013160200A1 Application of 18-methyl-15ss,16ss-methylene-19-nor-20-spirox-4-en-3-one systems in the treatment of menorrhagia, as well as intrauterine systems containing 18-methyl-15ss,16ss-methylene-19-nor-20-spirox-4-en-3-one for treating uterine bleeding disorders The present invention describes the intrauterine application of 18-methyl-15ß, 16ß-methylene-19-nor-20-spirox-4-en-3-one systems of the general formula (1), where R6 and R7 denote hydrogen or a methylene group, for the treatment of menorrhagia, generally uterine bleeding, as well as an intrauterine system for the stated application containing a compound of formula (1).
US20110118266 Derivatives of triazines and uracils, their preparation and their application in human therapeutics The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R1 represents: •a hydrogen or a linear or branched C1-C5 alkyl radical or, •a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, •a C6 2-oxocycloalkyl radical—R2 represents a methyl or heptyl, —m, n are equal to 1, —V represents CH2, —X—Y represents —N— (C═O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.
WO2009069352A1 Antimicrobial agent and external preparation for skin containing the same It is intended to provide a novel antimicrobial agent having a high safety, an excellent compounding property, and a potent antimicrobial activity. It is characterized by containing ricinoleic acid monoglyceride or diglyceryl ricinoleate monoester as an active ingredient. The antimicrobial agent of the invention is preferred as a compounding component of an antibacterial objective selected from foods, food packing materials, tableware, fragrances, cosmetics, external preparations for skin, skin washing agents, disinfectants, external lotions, hair agents, sterilization wipes, pharmaceuticals, quasi drugs, and oral health materials.
CN1757389A Implanted agent for preventing and treating biabetic retinopathy An implant for preventing and treating diabetic retinosis is composed of the medicine and the carrier. Said medicine is calcium hydroxyphenyl sulfonate.
EP2648760A2 Smart polymeric nanoparticles which overcome multidrug resistance to cancer chemotherapeutics and treatment-related systemic toxicity Polymeric nanoparticles with a hydrophobic core that encapsulates curcumin and a hydrophilic shell with one or more chemotherapeutic agents (e.g., doxorubicin) associated with the shell surface are formed from N-isopropylacryl amide (NEPAAM), acrylic acid (AA), and at least one vinyl monomer selected from the group consisting of vinyl acetate, 4-vinyl benzoic acid, methylmethacrylate, vinylmethacrylate, N-vinylpyrrolidone, N-vinyl piperidone, N-vinyl caprolacum, N-vinyl carbazole, and styrene, where the NIPAAM, the AA, and the vinyl monomer are present at molar ratios of 50-70:10-30:10-30 for NIPAAM:AA:vinyl monomer. These nanoparticles effectively overcome multidrug resistance and ameliorate cardiomyopathy in vivo.
US7449493 N-[2-[[1-[[[(2,4-dimethylphenyl)methyl]amino]methyl]cyclohexyl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide; monocyte chemoattractant proteins receptor antagonists or partial agonists/antagonists; antiinflammatory agent, autoimmune diseases; rheumatoid arthritis, multiple sclerosis, atherosclerosis The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
CN101805334A Lamivudin stearate and synthesis method and application The invention provides lamivudin stearate. The lamivudin stearate is characterized in that the lamivudin stearate is synthesized through lipophilicity modification of lamivudin, which is favorable for medicinal loads of targeted carrier materials; chitosan-stearate graft micelles having efficient cell intake and low toxicity are used for encapsulating antiviral medicaments of molecular targets incells so as to greatly increase medicament intake of viral cells and medicament concentration at the medicinal molecular targets; the increased medicament intake of the viral cells is favorable for reducing the distribution of the medicaments in normal tissues or cells and toxic and side effects of the medicaments; the increased medicament concentration at the medicinal molecular targets is favorable for improving the effects of the antiviral medicaments; and the lamivudin stearate can be applied to preparing the medicaments having efficient anti-HBV activity. The lamivudin stearate has the following chemical structural formula.
WO2005097151A1 Antioxidant composition and products containing the same An antioxidant composition containing a lutein ester and a black rice extract. It is preferable that the ratio of the mass of the lutein ester WL to the mass of the black rice extract WP, i.e., WL/WP is 0.2 or more but not more than 5. It is also preferable that the sum of the mass of the lutein ester WL and the mass of the black rice extract WP, i.e., (WL+WP) amounts to 0.1% by mass or more but not more than 50% by mass of the whole antioxidant composition. A food and a tablet preparation containing the antioxidant composition as described above.
US20100234426 Phenylpropionamide Compounds and the Use Thereof The invention relates to phenylpropionamide compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, B, R1, R2, R3, R4 and R5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the activation of opioid receptors, particularly μ-opioid receptors. Compounds of the present invention are especially useful for treating pain.
CN101164553A Application of jin mushroom polysaccharide germanium in preparing medicine for inhibiting H5N1 avian influenza virus The present invention discloses a new application of long-rooted mushroom polysaccharide germanium in preparation of medicine for inhibiting H5N1 subtype high-pathogenicity avian influenza virus. The invented pharmacodynamic experiments show that the long-rooted mush room polysaccharide germanium can effectively inhibit the propagation of H5N1 subtype high pathogenicity avian influenza virus in MDCK cell, so that the invented long-rooted mushroom polysaccharide germanium has obvious inhibition action for H5N1 subtype high pathogenicity avian influenza virus.
CN1939514A Ointment for treating orolingual wound promotion An ointment for treating orolingual sore or ulcer is prepare through pulverizing dogwood fruit, sieving, mixing part of the powdered bogwood fruit with black plum, decocting, filtering, laying aside, taking supernatant, vacuum concentrating, mixing it with the rest of powdered dogwood fruit, adding the extract of round cardamom, stirring, pulverizing, adding chlorpheniramine powder and phelodendron bark powder, and immersing in the solution of sodium alginate.
CN1850066A Carboplatin venous emulsion and its preparing method The present invention relates to a compound for venous transfusion. Said compound is characterized by that the carboplatin can be added into its stable oil-in-water emulsion. Said compound includes carboplatin, oil, water and surfactant. Besides, said invention also provides its preparation method.
CN1876084A Ointment for orthopedics The invention relates to an adhesive plaster for treating orthopaedic diseases which is prepared from the following raw materials (by weight portion): drynaria 30-60 parts, borax 30-60 parts, dragon's blood resin 40-60 parts, frank incense 30-50 parts, myrrh 30-50 parts, Chinese angelica root 50-80 parts, dipsacus root 50-60 parts, native copper 50-60 parts, momordica seed 30-50 parts, rheum officinale 30-50 parts, notoginseng 30-40 parts, buck grass 30-50 parts, Clematis chinensis 20-35 parts and speranskia herb 10-30 parts.
WO2011065420A1 Method for manufacturing a 6-substituted-1-methyl-1h-benzimidazole derivative, and manufacturing intermediate from said method Provided is a novel method for manufacturing a 6-substituted-1-methyl-1H-benzimidazole derivative. Also provided is a manufacturing intermediate from said method. The provided method, which manufactures a 6-substituted-1-methyl-1H-benzimidazole derivative represented by general formula (IV) (in which R3 represents a hydrogen atom or a C1-4 alkyl group), is characterized by: manufacturing a 4-substituted-N2-methylbenzene-1,2-diamine derivative from a specific 5-substituted-N-methyl-2-nitroaniline derivative; reacting same with {4-[(2,4-dioxo-1,3-thiazolidine-5-yl)methyl]phenoxy} acetate or an oxychloride or mixed acid anhydride thereof; and then performing intramolecular dehydration/condensation.
US20090099161 Substituted Imidazoquinolines and Imidazonaphthyridines Imidazoquinolines and imidazonaphthyridines with a substituent containing a functional group, e.g., an amide, sulfonamide, urea, or heterocyclyl group, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
CN102342960A Veterinary medicine composition for treating skin disease of fragrant pig The invention discloses a veterinary medicine composition for treating a skin disease of a fragrant pig. The veterinary medicine composition is characterized by consisting of the following parts of components by weight: 200-1000 parts of antitoxic 007, 1000-5000 parts of circolin, 100-500 parts of binotal, 100-300 parts of venenum bufonis, 10-100 parts of tiamulin fumarate soluble powder, 100-300 parts of lihao, 100-400 parts of BMK and 200-1000 parts of florfenicol. The veterinary medicine composition for treating the skin disease of the fragrant pig is mixed in feed in a certain proportion to feed the fragrant pig with agnogenic skin and breathing comprehensive symptoms, and the symptoms can be bettered after 15 days, and are not easy to reappear after being healed.
CN1887270A Nanometer berberine hydrochloride emulsion and its prepn process The present invention discloses one kind of nanometer berberine hydrochloride emulsion. The nanometer berberine hydrochloride emulsion consists of berberine hydrochloride 0.1-2 wt%, surfactant 20-40 wt%, co-surfactant 10-20 wt%, solvent 1-10 wt%, oil phase 5-30 wt%, sweetener 1-5 wt% and distilled water 27.5-70 wt%. The nanometer berberine hydrochloride emulsion has raised berberine hydrochloride dissolubility, raised bioavailability, lowered toxic side effect, simple preparation process and low production cost.
WO2011112156A1 Anti-cancer agent delivery vehicles capable of improved laoding There is provided a conjugate of a delivery agent containing a chemical moiety and at least one flavonoid. The flavonoid exists in a monomeric form or dimeric form before conjugation and remains in the monomeric form or dimeric form after conjugation. Preferably, the conjugate comprises two flavonoids. The delivery agent is conjugated at the C6 and/or the C8 position of the A ring of the flavonoid. An anti-cancer agent delivery vehicle comprising an anti-cancer agent and the conjugate is also provided.
US20100022472 Liquid, eye-instillable preparations comprising sodium hyaluronate A liquid, eye-instillable preparation comprises a viscosity-enhancing agent comprised of one or both of sodium hyaluronate and chondroitin sulphate, a preservative comprised of polyhexanide, and one or more carriers in which the agent and the preservative are dispersed.
US20050261163 Pharmaceutical products, preparation and uses thereof A pharmaceutical product comprising at least one therapeutic agent, whereby a unit dose of said therapeutic agent as provided by said pharmaceutical product can be administered to a patient during the passage of said therapeutic agent through the gastrointestinal tract of the patient, wherein said therapeutic agent is characterised as having an aqueous solubility of not greater than about 1 in 30 to 1 in 100, weight/volume, when measured at a temperature in the range of 15 to 25° C.
CN101869709A Composite of peptic ulcer resisting medicaments and preparation method thereof The invention discloses a composite of peptic ulcer resisting medicaments and a preparation method thereof, wherein troxipide as an active component and other peptic ulcer resisting medicaments form a composite preparation, and the weight ratio of troxipide and other peptic ulcer resisting medicaments is 1:0.05-1:50. The composite preparation can be used for treating gastric ulcer, duodenal ulcer, acute and chronic gastritis, gastroesophageal reflux diseases, functional dyspepsia diseases and the like. The invention provides the composite preparation which is superior to single medicament, has good therapeutic effect and consists of troxipide and other peptic ulcer resisting medicaments.
US20080269215 Bisamide Inhibitors of Hedgehog Signaling The invention provides inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein ring A, ring B, R1, R2, R3, R4, R5, m and n are as defined herein.
CN1660865A Saponin compound, general saponin of cynanchum bunaei and application in medication for treating disease of gstrointestinal tract 7 C12 steroid saponins including white fleeceflower glucosides A, B and C, white fleeceflower neoglucosides A and B, etc, and their mixture is prepared from white fleeceflower root. They can be used to prevent and treat gastrosis, gastric ulcer and duodenal ulcer.
US20130034610 Hydrophobic nanotubes and nanoparticles as transporters for the delivery of drugs into cells Methods and materials for delivering biologically active molecules to cells in vitro or in vivo are provided. The methods and materials use carbon nanotubes or other hydrophobic particles, tubes and wires, functionalized with a linking group that is covalently bound to the nanotubes, or, alternatively, to the biologically active molecule, such as a protein. The biologically active molecule is preferably released from the nanotube when the complex has been taken up in an endosome.
WO2008001931A3 Fused cyclic compounds The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.
US7196103 Indole derivatives as factor Xa inhibitors The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.
WO2005027889A1 Visceral pain dulling composition A method of dulling visceral pain, comprising administering civetone to patients suffering from visceral pain, characterized in that the administration is performed by means for transmitting civetone stimulation through the olfactory nerve to the brain. In this method, the visceral pain dulling effect can be exerted in a short period of time, and further, since blood is not intermediacy, the visceral pain can be dulled without any side effects on the liver and kidney.
WO2014000027A1 Prevention and treatment of haematological conditions The present invention relates generally to methods for the prevention and treatment of haematological conditions that exhibits elevated levels of free immunoglobulin light chains (FLCs), including multiple myeloma, B-cell lymphomas, and associated diseases and conditions.
WO2012100383A1 Refining process of cefamandole sodium Provide a process of refining cefamandole sodium comprising steps as follows: step 1), adsorbing cefamandole sodium by strong acid ion exchange resin, and collecting the eluant after eluting, then decompressing and concentrating to obtain cefamandole acid, step 2), using sodium hydroxide solution or alkaline sodium solution to neutralise and adjust pH, filtering while the solution is hot to remove insoluble material, then obtain cefamandole sodium solution; step 3), adding ethanol into the solution with a water/ethanol volume ratio of 4:6, and controlling the temperature to recrystallization, acquiring purified cefamandole sodium. The refined cefamandole sodium has a purity higher than 99.5%, most of which has a purity higher than 99.6%, and the refined cefamandole sodium has very low heavy metal content.
CN101756948A Composition of ambroxol hydrochloride and arginine and preparation method thereof The invention belongs to the technical field of medicine, in particular to a composition of ambroxol hydrochloride and arginine and a preparation method thereof. The weight ratio of the ambroxol hydrochloride and the arginine in the composition is 1:0.01 to 0.8. The invention also provides a preparation method of freeze-dried powder preparation of the composition, and a use of the composition in the preparation of expectorant drugs.
DE102005009217A1 New phosphoric acid salts of 6-dimethylaminomethyl -1-(3-methoxyphenyl)-1,3-dihydroxycyclohexane useful to treat e.g. pain, migraine, depressions, neurodegenerative illnesses, cognitive illnesses, fear conditions and epilepsy Phosphoric acid salt of 6-dimethylaminomethyl-1-(3-methoxyphenyl)-1,3 -dihydroxycyclohexane compound (I) (where the phosphoric acid is preferably diphosphoric acid and/or orthophosphoric acid), is new. Phosphoric acid salts of 6-dimethylaminomethyl-1-(3-methoxyphenyl)-1, 3-dihydroxycyclohexane compound of formula (I) (where the phosphoric acid is preferably diphosphoric acid and/or orthophosphoric acid), are new. R2>, R3> = OH or H. Independent claims are also included for: (1) preparation of (I); (2) polymorph A of (I) in the orthophosphate salt form having X-ray powder diffraction (XRPD) as given in the specification and measured with copper potassium (CuK) alpha radiation or by a Raman spectrum with excitation wavelength of 1064 nm as given in the specification; (3) polymorph B of (I) in the orthophosphate salt form having XRPD as given in the specification and measured with CuK-alpha radiation or by a Raman spectrum with excitation wavelength of 1064 nm; (4) polymorph C of (I) in the orthophosphate salt form having XRPD as given in the specification of table 3 and measured with CuK-alpha radiation or by a RAMAN spectrum with excitation wavelength of 1064 nm as given in the specification; (5) polymorph amorphous (I) in the orthophosphate salt form having XRPD as given in the specification and measured with CuK-alpha radiation, and (6) preparation of one or more polymorphs. [Image] - ACTIVITY : Analgesic; Antimigraine; Antidepressant; Neuroprotective; Nootropic; Antiparkinsonian; Anticonvulsant; Tranquilizer; Antitussive; Uropathic; Antidiarrheic; Antipruritic; Neuroleptic; Cerebroprotective; Vasotropic; Immunomodulator; Anabolic; Eating-Disorders-Gen.; Antialcoholic; Antiaddictive; Gastrointestinal-Gen. No biological data is given. - MECHANISM OF ACTION : None given.
US20080113973 Pharmaceutical composition in unit dose form which contains a COX-2 inhibitor and a thromboxane A2 receptor antagonist; for treatment of pain or inflammation; less risk of inducing adverse cardiovascular effects than when COX-2 inhibitors are administered alone The invention is directed to methods and compositions that can be used in the treatment of inflammation, pain and cardiovascular disorders. Methods and compositions are described involving the combination of a thromboxane A2 receptor antagonist and an inhibitor specific for cyclooxygenase-2.
CN101579341B Novel use of pantoprazole sodium in treatment of cholecystitis The invention discloses novel use of pantoprazole sodium in treatment of cholecystitis. The invention also discloses an intravenously administrable pantoprazole sodium injection and a preparation method thereof.
CN103316242A Compound medicine for treating hyperostosis caused by weakness of spleen and stomach and preparation method thereof The invention discloses a compound medicine for treating hyperostosis caused by weakness of spleen and stomach. The compound medicine is prepared from the following crude drugs: domperidone, astragalus membranaceus, beautiful millettia root, philippine flemingia root, cooked adix polygoni multiflori, fried placenta, flying ginseng, oyster, cuttlebone, tenodera aridifolia stoll, citrus chirocarpus, schefflera arboricola, fried hawthorn, fried rice sprout, stir-baked mass fermentata medicinalis, fried rhizoma atractylodis, fried hyacinth bean, pericarpium citri reticulatae, pseudo-ginseng, root of red-rooted salvia and honey-fried licorice root. The medicine disclosed by the invention is significant in treatment effect on the hyperostosis caused by weakness of spleen and stomach, high in recovery rate, and convenient to take; the effective rate is 96.6%; the recovery rate is 90%; and the hyperostosis does not reappear after being cured.
EP1626973B1 (1s,5s)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane is an effective analgesic agent The present invention discloses (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane and its use to treat pain and other disorders associated with the nicotinic acetylcholine receptor.
US20100240732 Aptamer-targeted sirna to prevent attenuation or suppression of a t cell function Compositions for countering immune attenuating/suppressive pathways comprise targeting agents or aptamer targeted RNAi-mediated gene silencing (siRNA/shRNA). These compositions have broad applicability in the treatment of many diseases.
CN103623394A Application of PEG-HM-3 and platinum, taxol or Emtriva medicines to preparation of solid tumor medicines The invention discloses application of PEG-HM-3 and platinum, taxol or Emtriva medicines to preparation of solid tumor medicines, and belongs to the field of medicines for treating tumors. The PEG-HM-3 is polyethylene glycol modified polypeptide HM-3 with the molecular weight range of 10,000 to 40,000; and the platinum, taxol or Emtriva medicines serving as active components and auxiliary acceptable medicinal carriers are prepared into various pharmaceutically acceptable preparations. According to a large amount of experiments, an integrin blocking agent PEG-HM-3 has a definite target spot and is reasonably used in combination with platinum, taxol or Emtriva, so growth of tumors such as lung cancer, liver cancer, gastric cancer, breast cancer, cervical cancer, ovarian cancer and intestinal cancer can be effectively inhibited. The medicines are combined to serve as a medicine, so tumors can be treated effectively, medicine combination is scientific, reasonable, practical and effective, the treatment spectrum of tumor treatment is greatly enlarged, the toxic or side effect is reduced, and obvious social value and market value are achieved.
US20120220518 Therapeutic agent delivery system and method A therapeutic agent delivery system includes a therapeutic agent delivery platform and a therapeutic guest agent. The therapeutic agent delivery platform is capable of being implanted in a tissue being treated. The platform includes a substrate and at least one host molecule coupled to the substrate. The therapeutic guest agent is capable of reversibly coupling with the host molecule when administered to the tissue being treated. The reversible coupling is defined by the binding affinity between the host molecule and the therapeutic guest agent. The therapeutic guest agent is delivered at a rate determined by the affinity release rate between the host molecule and the therapeutic guest agent. The degradation rate of the therapeutic guest agent may be slower than the affinity release rate between the host molecule and the therapeutic guest agent.
EP2308509A1 Inhibitor of analgesic tolerance Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.
WO2009109401A1 Salts of memantine and cox-inhibitors and their crystalform in the treatment of pain The present invention relates to salts of Memantine and COX-INHIBITORs, their crystal form, the processes for preparation of the same and their uses as medicaments, more particularly for the treatment of pain.
US20100298285 Biclycloheteroaryl Compounds as P2x7 Modulators and Uses Thereof Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
US8753665 Controlled delivery system The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided. Preferably the composition contains bupivacaine and a sugar ester such as saib.
WO2005000288A2 Treatment of protein aggregation disorders The present invention is based, at least in part on the discovery of therapeutic agents capable of preventing, inhibiting or modulating abnormal processing, misfolding or aggregation of protein. The therapeutic agents of the invention may prevent, inhibit or modulate the formation of inclusions. The therapeutic agents of the invention may also be capable of facilitating clearance and/or blocking the cellular toxicity of inclusions to treat or ameliorate disorders characterized by protein aggregation. Compounds which bind to structural motifs commonly found in protein aggregates, such as ß-sheets, would represent strong candidates for such compounds and are therefore desirable.
US20120302613 Novel antibiotics The invention relates generally to novel antibiotics and their analogs, to processes for the preparation of these novel antibiotics, to pharmaceutical compositions comprising the novel antibiotics; and to methods of using the novel antibiotics to treat or inhibit various disorders.
US20110301169 Therapies for Treating Cancer Using Combinations of COX-2 Inhibitors and Antimetabolites A method for treating a subject having cancer, comprising administering to the subject, a therapeutically effective amount of a combination comprising a 1,2-diphenylpyrrole derivative or the respective pharmaceutically acceptable salt, solvate, polymorph or prodrug and an anti-metabolite.
CN101352435A Use of lipoamide for preventing and treating age related macular degeneration The invention belongs to the field of pharmacy, disclosing a novel purpose of lipoamide which is used for preparing a preparation for preventing or curing diseases being relevant to cell trauma. The invention discloses the novel purpose at the aspect of preventing and curing cell trauma for the first time; in addition, the extremely effective easing and curing function of the lipoamide to the trauma of retinal pigment epithelium cell is disclosed for the first time, the pharmacological actions are very obvious, no any toxic and side effects appear and the admirable medicated prospect can be reached.
DE102004022383A1 New pyridopyrazine derivatives are modulators of kinase activity, useful for the treatment of diseases associated with abnormal cellular signaling, e.g. tumors Pyrido[2,3-b]pyrazine derivatives (I) their salts, derivatives, analogs, solvates, hydrates and polymorphs, as racemates and as pure or mixed enantiomers and/or diastereomers or tautomers are new. Pyrido[2,3-b]pyrazine derivatives of formula (I) their salts, derivatives, analogs, solvates, hydrates and polymorphs, as racemates and as pure or mixed enantiomers and/or diastereomers or tautomers are new. [Image] R1 and R2 : hydrogen, hydroxy, halo, 1-8C alkyl, aryl (optionally substituted by one or more Q1), heteroaryl (optionally substituted by one or more Q2), OR5, SR6, or NR7R8; one of R3 and R4 : hydrogen and the other is NR9R10; R9 : hydrogen, alkyl (A), cycloalkyl (Cy), heterocyclyl (Hc), aryl (Ar), heteroaryl (Ha) (the last 4 optionally substituted by alkyl), and all these groups may themselves be substituted; R10 : -CYNR11R12, -CY1NR13R14 or -C(NH)R16; Y : oxygen or sulfur; R11 and R12 : hydrogen, A (optionally substituted by Q4), Cy (optionally substituted by Q5), Hc (optionally substituted by hydroxy, alkoxy, aryloxy, amino(itself optionally substituted by A, Ar), A, alkyl-Ar or Ar), Ar (optionally substituted by Q6), Ha (optionally substituted by Q7), COR17, or R11 and R12 together form Cy or Hc; Y1 : NH; R13 and R14 : hydrogen, A (optionally substituted by Q8), Cy (optionally substituted by Q9), Hc (optionally substituted by hydroxy, alkoxy, aryloxy, amino (itself optionally substituted by A or Ar), A or Ar), Ar (optionally substituted by Q10), Ha (optionally substituted by Q11), or R13 and R14 together form Cy or Hc; R16 : A (optionally substituted by Q12), Cy (optionally substituted by Q13), Hc (optionally substituted by hydroxy, alkoxy, aryloxy, amino (itself optionally substituted by A or Ar), A or Ar), Ar (optionally substituted by Q14) or Ha (optionally substituted by Q15). The full definitions are given in the DEFINITIONS (Full Definitions) Field. - ACTIVITY : Cytostatic; Vasotropic; Antipsoriatic; Antiarteriosclerosis; Hepatotropic. - MECHANISM OF ACTION : Tyrosine or serine/threonine kinase modulator. 1-allyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea (Ia) had IC50 for inhibition of phosphorylation by the c-Raf-Mek-Erk cascade of about 1 MicroM.
CN101805340A Beta-chain simulative and correlation method thereof The invention discloses a structure limited compound for simulating a beta-chain region secondary structure of a biological active peptide and a protein. The beta-chain simulative structure is applied to being used as a diagnosis agent and a treating agent in a wide field. The invention also discloses a library containing the beta-chain simulative structure and a method for screening the beta-chain simulative structure to identify the bioactive member.
CN102018722A Ointment for curing trauma The invention discloses ointment for curing trauma, which comprises the following raw medicinal materials in part by weight: 250 parts of sulfanilamide, 3 parts of cinnabar and 6 parts of borneol. A method for preparing the ointment comprises the following steps of smashing the cinnabar and the borneol and then mixing the smashed materials and sulfanilamide. The ointment is a compound preparation and has the effects of promoting tissue regeneration, preventing corrosion, diminishing inflammation, relieving pain and promoting healing of wounds, and cures wounds and various traumas through external application. The ointment for curing trauma has the characteristics of quick response, good curing effect, no toxic or side effect, and quick promotion on wound skin coalescence.
US20060257882 Novel polynuceotides and polypeptides encoded thereby This application is drawn to novel nucleic acid sequences encoding mammalian polypeptides that have sequence similarity to human breast tumor-associated protein 47. The nucleic acid sequence is 1987 nucleotides long and contains an open reading frame from nucleotides 991 to 1447. The novel, encoded polypeptides comprise 152 amino acid residues.
WO2014078801A1 Methods and compositions comprising guanidines for treating biofilms Methods of treating or reducing biofilms, treating a biofilm-related disorder, triggering biofilm disassembly, and preventing biofilm formation using guanidines is described.
CA2177578C Preventing and treating elevated intraocular pressure associated with administered or endogenous steroids using non-steroidal cyclooxygenase inhibitors Methods and compositions for preventing or treating non-inflammatory elevated intraocular pressure associated with administered or endogenous steroids including administering to a mammalian organism a composition including (a) an ophthalmologically effective amount of non-steroidal cyclooxygenase inhibitor, and (b) a pharmaceutically acceptable carrier, to reduce or prevent an elevation of intraocular pressure and/or protein marker induction induced by chronic exposure to glucocorticoids.
US7629313 Immunomodulatory polymeric antigens for treating inflammatory pathologies Provided are natural and synthetic immunomodulatory polymeric antigens (SPAs), compositions containing SPAs, and methods of using these natural and synthetic SPAs and compositions to prevent or treat inflammatory pathologies.
US20100087534 Use of a Photosensitizing Agent in the Treatment or Prevention of an Inflammation-Associated Disorder in the Gastrointestinal Tract of a Mammal The present invention relates generally to the field of Photodynamic therapy (PDT) and more particularly to the use of a photosensitizing agent for the preparation of a medicament for the treatment or prevention of an inflammation-associated disorder in the gastrointestinal tract of a mammal, wherein the expression of pro-inflammatory markers in a tissue of said gastrointestinal tract is decreased after administering said photosensitizing agent to said tissue and exposing said tissue to a light having a wavelength absorbed by said photosensitizing agent.
CN103550761A Cream for wound surface and preparation method thereof The invention discloses a cream for a wound surface and a preparation method thereof. The cream comprises coconut oil, a self-emulsifying compound emulsifier AC-402, alpha-chymotrypsin, lidocaine, glycerin, carbomer, triethanolamine, an ethanol solution of ethylparaben and distilled water. Compared with the prior art, the cream prepared in the invention has the following advantages: the cream comprises alpha-chymotrypsin and lidocaine, and the cream has appropriate viscosity and good coating and spreading performance, is fine and uniform and can clean wound surfaces, eliminate suppurative exudate and necrotic tissue, promote growth of newborn granulation, accelerate healing, mitigate pains and substantially improve compliance of patients, wherein the elimination rate of necrotic tissue reaches more than 90%.
US20080305163 Butylphthalide soft gel capsule and its preparation procedure The present invention discloses a novel dosage form of butylphthalide soft capsule and its preparation procedure. Butylphthalide soft capsule is composed of a coating material and a drug-containing oil. The drug-containing oil is basically composed of butylphthalide and diluent—vegetable oil, wherein the weight ratio of butylphthalide to oil ranges from 1:0˜10. The coating material is composed of gelatin, plasticizer and water, wherein the weight ratio of gelatin to plasticizer to water is in the range of 1:0.2˜0.4:0.8˜0.3. The butylphthalide soft capsule described in this invention can mask the strong and specific flavor of butylphthalide, and overcome the difficulties associated with formulating oily active agents into other oral preparations. The disintegration time of the soft capsule complies with the requirement of Pharmacopoeia of P.R. China.
US7238675 consisting of a substantially uncharged antisense oligomer with ratio of uncharged linkages to charged linkages in the oligomer is at least 4:1, preferably at least 5:1, and more preferably at least 8:1 The invention relates to compositions comprising oligomers antisense to bacterial 16S or 23S rRNA and capable of selectively modulating the biological activity thereof, and methods for their use. More particularly, the invention relates to antisense oligomers directed to 16S or 23S rRNA found in one or more particular bacteria, or generally conserved among bacteria in general, and to pharmaceutical compositions and methods of treatment comprising the same.
US20130053441 Novel ester derivative and use thereof A compound represented by the following formula (I′) wherein X1 is a methylene group, an ethylene group, a trimethylene group or a vinylene group, X2 is a divalent group represented by the following formula A or B, Y is an ethylene group or a vinylene group, m and n are each an integer of 0 to 7, which satisfy m+n=0 to 8, R1 and R2 are each independently a hydrogen atom, a methyl group or an ethyl group, provided that when X1 is a methylene group, then X2 is not a divalent group represented by the formula A, and when X1 is a vinylene group, then X2 is not a divalent group represented by the formula A. The compound is a stable capsinoid derivative, and is useful as an active ingredient of an external blood circulation enhancer or a cosmetic composition, a pharmaceutical composition, or a food composition.
CN101703470B Solid preparation of fluconazole liposome and new application thereof The invention provides a solid preparation of fluconazole liposome and a new application thereof. Specifically, the solid preparation of the fluconazole liposome is prepared by the fluconazole liposome and auxiliary materials. The invention discovers unexpectedly that when fluconazole and specific phospholipid and cholesterol are mixed in a certain matching ratio and combined with an antioxidant to prepare the liposome, and the problems about stability and dissolution rate of the solid preparation of the fluconazole liposome and the like are resolved. The liposome technique has high entrapment rate and good product quality and can be used for treating mucormycosis.
US6955815 Combinations for the treatment of inflammatory disorders The invention features a pharmaceutical composition that includes amoxapine and a corticosteroid.
CN101467967B Double-element solution type preparation for intravenous injection and intracerebral injection The invention discloses a binary solution type formulation for intravenous and intracerebral injection. The main active component thereof is temozolomide with the binary system and having temozolomide sterile powder and solvent for dissolving medicaments. The operating temozolomide solution agent can be obtained through the combination of the solvent. The invention is characterized in that, 1, the binary formulation is stable at the room temperature for over 2 years; 2, the prepared medicaments liquid is stable at the room temperature at least for 48h to meet the operating requirement of injection administration; 3, the solvent is nontoxic and non-irritant, and the prepared medicaments can be used for the intracerebral injection during the operation and stereotaxic intraturmor injection of local chemotherapy.
WO2011137503A1 Methods for preparing ruthenium phosphine complexes with a structure containing picolinate and/or diimine and/or biphosphine ions, ruthenium phosphine complexes obtained by these methods and uses thereof The invention relates to the synthesis and characterisation of ruthenium(II) phosphine complexes containing picolinate and/or diimine and/or biphosphine ions and having an outstanding pharmacological activity for inhibiting the growth of tuberculosis mycobacteria. These complexes can first be used in the chemical industry, and in the medium and long term, in the pharmaceutical industry. The invention also describes how the activity against tuberculosis bacillus was determined, and how the toxicity of the complexes against macrophage cells within which the tuberculosis bacillus grows was assessed.
CA2575790A1 The use of a modafinil compound for the treatment of problem gambling The invention is directed to methods for the treatment of problem gambling, impulse control disorders, and/or disorders for which boredom proneness and/or impulsivity are prominent risk factors. The method comprises the administration of a modafinil compound to a patient in need of such treatment. The invention also discloses the use and methods of use of a modafinil compound for the reduction of the primed motivation to gamble, decrease of the reinforcing effect of gambling, reduction of enjoyment of slot machine gambling, production of improvement in inhibitory control following the gambling episode, and production of a more rapid adoption of a low risk gambling strategy.
US20050085509 KInase inhibitors; antiarthritic agents; autoimmune diseases; sepsis; cachexia; Alzheimer's disease; antihistamines; thrombosis; glomerulonephritis; inflammatory bowel disorders; crohn's disese; multiple sclerosis; antitumor agents; skin disorders A piperidin-2-one derivative compound represented by formula (I): wherein all symbols are described in the specification, or a non-toxic salt thereof. The compound represented by formula (I) inhibits activation of p38MAP kinase, and is useful for prevention and/or treatment of various inflammatory diseases, rheumatoid arthritis, osteoarthritis, arthritis, osteoporosis, autoimmune diseases, infectious diseases, sepsis, cachexia, cerebral infarction, Alzheimer's disease, asthma, chronic pulmonary inflammatory diseases, reperfusion injury, thrombosis, glomerulonephritis, diabetes, graft versus host rejection, inflammatory bowel disease, Crohn's disease, ulcerative colitis, multiple sclerosis, tumor growth and metastasis, multiple myeloma, plasma cell leukemia, Castleman's disease, atrial myxoma, psoriasis, dermatitis, gout, adult respiratory distress syndrome (ARDS), arteriosclerosis, post-percutaneous transluminal coronary angioplasty (PTCA) restenosis or pancreatitis.
WO2011018580A1 Chromium and yeast beta-glucan compositions for preventing and/or treating diabetes The present invention relates to a composition for preventing and/or treating diabetes, and to a food composition having beneficial effects in preventing and/or treating diabetes. The present invention further relates to the use of such a composition as a drug for preventing and/or treating hyperglycemia, hyperinsulinemia, type 1 diabetes, and/or type 2 diabetes.
US20110269726 Method of and system for treatment of inflammatory skin conditions For treating inflammatory skin conditions a treatment cream including hydrocortisone is applied on a skin; and the applying the treatment cream is combined with treatment of the skin with moisturizer with a moisturizer.
US7220760 1-carbonyl-4-carbonylaminotetrahydroquinoline derivatives; especially treating asthma and allergic rhinitis The invetion relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the description, their use as medicament, pharmaceutical compositions containing them and processes for their preparation.
CN1857265A Slow released omeprazole/domperidone preparation and its preparing process and application The present invention provides slow released omeprazone/domperidone preparation and its preparation process and application. The slow released omeprazone/domperidone preparation has less blood medicine concentration fluctuation, reduced medicine taking times, raised curative effect and lowered toxic side effect.
US8513220 Aromatic compounds having sphingosine-1-phosphonate (S1P) receptor activity Novel aromatic compounds which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
CN101953910B Coptis alkaloid and ferulic acid compound with glucose-lowering effect The invention discloses a coptis alkaloid and ferulic acid compound with glucose-lowering activity, which comprises the following components in percentage by weight: 0.1 to 99.9 percent of coptis alkaloid and 0.1 to 99.9 percent of ferulic acid, wherein the coptis alkaloid contains berberine or coptisine or palmatine or jatrorrhizine or the sum of four coptis alkaloids, or is total coptis alkaloids extracted from coptis. The compound has the advantages of better glucose-lowering effect compared with that of the coptis alkaloid or ferulic acid, and obvious glucose-lowering effect according to administration in a dosage of 0.5 to 5 grams every person per day.
US20110280886 Treating cancer by modulating mnk The present invention relates to a method for treating cancer in a subject using a mTOR inhibitor in combination with a therapeutically effective amount of a modulator of a MNK.
CN102321142A Abiraterone acetate crystal form and preparation method thereof The invention relates to a new crystal form of a medicament, namely abiraterone acetate for treating prostatic cancer and a preparation method thereof, a pharmaceutical composition containing the new crystal form, and application of the new crystal form in preparing medicines for treating prostatic cancer.
CN103751171A Novel natural anticancer medicine prepared by using dihydromyricetin cooperated organic acids as raw materials The invention relates to a method for preparing a natural anticancer medicine by using dihydromyricetin cooperated organic acids as raw materials. The natural novel anticancer medicine is prepared by using dihydromyricetin (with the purity of 95% or more) cooperated lactic acid and citric acid as main raw materials, and dihydromyricetin is extracted from vine tea stem leaves; and the preparation method of the medicine comprises the following steps: dissolving dihydromyricetin in 68% ethanol, adjusting the mass concentratin of dihydromyricetin to 5g/L, sequentially adding 0.5mol/L of a lactic acid solution and 0.5mol/L of a citric acid solution to the obtained dihydromyricetin solution, fully mixing by using a 200rpm shaking bed at 25DEG C for 10min, and filtering by using filter paper to remove precipitates, and taking the obtained filtrate, wherein the addition amount of the lactic acid solution accounts for 0.6% of the total volume of the dihydromyricetin solution, and the addition amount of the citric acid solution accounts for 0.9% of the total volume of the dihydromyricetin solution. Results of in-vitro apoptosis experiments of prostate PC-3 cancer cells show that DMY (dihydromyricetin) has a substantial inhibition effect on the prostate PC-3 cancer cells, and the cooperation of dihydromyricetin, lactic acid and citric acid has a better inhibition effect on the prostate PC-3 cancer cells.
WO2011090005A1 Pharmaceutical preparation for colon cancer, and treatment method Provided are a treatment method and a pharmaceutical which combines a chemotherapeutic agent and a human anti A33 antibody for tumor of the colon which is difficult to be treated by surgery. Patients suffering from colon cancer which is deemed to be difficult to treat with conventional colon cancer treatment and or patients suffering from colon cancer and have relapsed under existing treatment can experience a constant antitumor effect by being subjected to the treatment method or by taking the pharmaceutical which combines a human anti A33 antibody and CPT-11 (irinotecan).
WO2008028324A1 Novel levamisole formulation for allergic rhinitis The use of levamisole in the manufacture of a medicament for the therapeutic treatment of allergic rhinitis, said levamisole is in the form of a nose drops spraying agent, aerosol, aerosol of micropowders for inspiration or nasal gel.
WO2008003396A1 Indazole derivatives for treating hsp90-induced diseases The invention relates to novel indazole derivatives of formula (I), in which R1- R3 are defined as cited in claim (1). Said derivatives are inhibitors of HSP90 and can be used to produce a medicament for treating diseases, in which the inhibition, regulation and/or modulation of HSP90 plays a role.
WO2010081783A1 Novel specific inhibitors of ubiquitin specific protease 7, the pharmaceutical compositions thereof and their therapeutic applications The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.
CN1934101B Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1', R1'', R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.
WO2014122530A1 Novel functionalized 4-(phenoxymethyl(-1,3-dioxolane analogs exhibiting cytochrome p450 inhibition and their method of use Embodiments of the present invention relate to 4-(phenoxymethyl)-1,3-dioxolane analogs and pharmaceutical compositions thereof having a disease-modifying action in the treatment of diseases associated with the overproduction of Cortisol that include metabolic syndrome, and any involving the overproduction of Cortisol.
CN1615856A Antiseptic composition of sodium ticarcillin for injection The antiseptic composition of sodium ticarcillin for injection consists of sodium ticarcillin and sodium tazobactam in the ticarcillin/tazobactam weight ratio of 1-32, preferably 1-12. Clinically, it is used in treating sensitive bacterium caused septicemia and bacteremia, abdominal cavity infection, hypoimmunity caused infection, respiratory infection, post-operational infection and many kinds of infections. The medicine has raised ticarcillin antiseptic activity and wide antiseptic spectrum.
EP2201897A2 Tumor targeted photodiagnostic-phototherapeutic agents Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.
WO2007142253A1 2-cyanopyrrolidine derivative Disclosed is a 2-cyanopyrrolidine derivative represented by the general formula [I] below or a pharmacologically acceptable salt thereof. Also disclosed are a method for producing the 2-cyanopyrrolidine derivative, a pharmaceutical composition containing the compound as an active ingredient, use of the compound for inhibiting the activity of DPPIV, and the like. [I] [In the formula, R represents (1) a morpholino, or (2) an optionally substituted piperazin-1-yl.]
WO2011054292A1 Certain crystalline hydrates, pharmaceutical compositions thereof and methods for preparation and use thereof At least one crystalline hydrate of (S)-[N-3-(3'-fluoro-4'-(4''-phenyl piperazinyl)) phenyl-2-oxo-5-oxazolidinyl] methyl acetamide, such as those with the following formula, wherein y is a number ranging from 1/12 to 1. Also provided are methods for the preparation of such crystalline hydrates, pharmaceutical compositions comprising such crystalline hydrates, and methods for their uses.
US20110044903 Methods for producing microbubbles The present invention provides methods for the preparation of gas-filled microbubbles, and methods of using for therapeutic and/or diagnostic applications. In particular, the methods of the invention allow for the preparation of gas-filled microbubbles having narrow size distributions and defined ultrasonic properties.
CN101307078A Galactosyl thiourea heterocyclic compounds, synthetic method thereof and antineoplastic applications The invention discloses a group of galactosyl thioureas heterocyclic compounds, a preparation method and biological activity thereof. The compounds are indicated by the following general formula. A B in the general formula is defined by an instruction book. The invention introduces a method for synthesizing the galactosyl thioureas heterocyclic compounds through six steps, which takes full acetic acid esterified galactosyl, bromine water, lead rhodanide, heterocyclic base, ethyl chloroacetate and hydrazine hydrate as raw materials, takes glacial acetic acid, trifluoroacetic acid, xylene, toluene, ethyl benzene, N,N- dimethyl formamide, dimethyl sulfoxide, dioxane, pyridine, methanol, ethanol, isopropyl alcohol, absolute methanol and absolute ethyl alcohol as solvents, and takes sodium hydride, anhydrous potassium carbonate and sodium methoxide as basic catalysts. The compounds have inhibiting effects on human body lung cancer cell strains and liver cancer cell strains.
CN101186605A 2-vinyl-8-hydroxyquinoline derivative, preparation method and application thereof The invention discloses a 2-vinyl-8-bioquin derivative, which preparation method comprises that 2-bioquin-8-bioquin and aromatic aldehyde are added into acetic anhydride to be dissolved, heated, refluxed and reacted at 120-140DEG C for 40-96h, the reaction product is separated and purified via column chromatography to obtain the pure 2-vinyl-8-bioquin derivative. The inventive 2-vinyl-8-bioquin derivative has significant oxidization resistance, better than strong antioxidant glutathione GSH which can eliminate free group. The inventive product can be used to prepare antioxidant, which further can accelerate the increment of mesenchymal stem cells in bone marrow, to prepare bone marrow mesenchymal increment accelerant.
WO2014001363A1 Novel tetrazole derivatives and their use as potassium channel modulators A tetrazole derivative of general formula (I), a pharmaceutical composition comprising said compound and its use for treating, alleviating or preventing diseases or disorders relating to the activity of potassium channels.
CN102133198A Ifenprodil tartrate freeze-dried powder injection and preparation method thereof The invention discloses an ifenprodil tartrate freeze-dried powder injection, and belongs to the technical field of medicine. The ifenprodil tartrate freeze-dried powder injection comprises the following raw materials: 2 to 10 weight parts of ifenprodil tartrate (C21H27NO2)2.C4H6O6 and 20 to 200 weight parts of excipients. The invention also discloses a preparation method of the freeze-dried powder injection. The ifenprodil tartrate freeze-dried powder injection prepared by the method only contains the excipients required by the freeze-dried powder injection, so that possible adverse reaction caused by the addition of other auxiliary materials is avoided. Besides, the ifenprodil tartrate freeze-dried powder injection is high in stability and convenient to store and transport.
CN103467409A Substituted tetrazole carboxylic acid compounds and application thereof The invention relates to the field of diabetes related medicines. The invention particularly relates to tetrazole-carboxylic-acid-containing compounds (disclosed as general formula I) capable of treating diabetes as a peroxisome proliferator-activated receptor (PPAR) agonist, and a preparation method and application thereof in treating diabetes. In the general formula I, the groups are defined in the specification.
CN1977882B Medicinal composition of astragalus, hypericum japonicum thunb. and tiopronin, and its preparing method The present invention discloses a medicine composition for curing hepatic diseases. Said medicine composition is made up by using (by weight portion) 400-1000 portions of astragalus root, 50-1000 portions of grangea maderaspatana and 5-80 portions of tiopronin, and can be made into oral preparation and injection. It mainly is used for curing viral hepatitis, medicamentous liver lesion, fatty liver and alcoholic hepatitis, etc.
CN102552294A Compound vitamin (3) freeze-dried powder injection for injection and preparation method and analysis method thereof The invention provides a compound vitamin freeze-dried powder injection for injection, which comprises vitamin B15-15 parts by weight, riboflavin sodium phosphate 3-8 parts by weight (counting by reducing crystal water), vitamin C 150-250 parts by weight, glycine 350-500 parts by weight and water for injection 1000-5000 parts by weight which is used as a solvent during preparation and is finally removed. The compound vitamin freeze-dried powder injection for injection is good in stability, high in safety and convenient to store and transport. The invention further provides a preparation method of the compound vitamin freeze-dried powder injection for injection. The compound vitamin freeze-dried powder injection for injection prepared through the preparation method is good in stability and high in safety. The invention further provides an analysis method of the compound vitamin freeze-dried powder injection for injection, and the analysis method is particularly specific to relevant substance of unstable basic medicines.
CN102648906A Application of sunitinib in preparation of acetylcholinesterase inhibitor The invention discloses an application of sunitinib in preparation of an acetylcholinesterase inhibitor. Sunitinib used as an antineoplastic agent in the prior art is applied to the preparation of the acetylcholinesterase inhibitor in the technical solution provided by the invention and is used as a medicine for treating the Alzheimer's disease.
US7432285 Nitrosated and nitrosylated cyclooxygenase-2 inhibitors, compositions and methods of use The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or optionally, at least one therapeutic agent. The present invention also provides novel compositions comprising at least one parent COX-2 inhibitor and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The present invention also provides kits and methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity; and for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2.
CN1839847A Tizanidine hydrochloride oral disintegrating tablet and preparation method thereof The invention discloses a Tizanidine hydrochloride orally disintegrating tablet, which comprises Tizanidine hydrochloride as the active ingredient, disintegrating agent, flavoring agent and other common acceptable adjuvant, wherein the content of Tizanidine hydrochloride in each tablet is 2-4mg. The invention also provides the process for preparing the tablet.
WO2010062261A1 System and method for preparing a controlled releas preparation A method for preparing a controlled release preparation. The method comprises forming a coating mixture, coating a core with the coating mixture for forming a hydrogel layer over the core. The method further comprises coating the hydrogel layer with hydrophobic polymers to form a hydrophobic layer over the hydrogel layer. The coating mixture if formed by blending an aqueous dispersion of Chitosan with a polysaccharide colloid composition. An active ingredient is added. The coating mixture is coated onto the core by fluidized bed technology. The hydrophobic polymer is also coated onto the hydrogel layer by fluidized bed technology. A system for preparing the controlled release preparation is also provided by the present invention. An exemplary controlled release preparation is also provided by the present invention.
CN102988847A Medicine composition used for treating vaginitis The invention relates to a medicine composition used for treating vaginitis, and belongs to the technical field of medicine. The medicine composition is composed of amur corktree bark, common cnidium fruit, sessile stemona root tuber, lightyellow sophora root, flatspine pricklyash, hairyvein agrimonia herb, borneol, and the like. The medicine composition has the functions of heat clearing, detoxifying, dampness eliminating, and disinfecting. The medicine composition is used in treating vaginitis, especially trichomonas vaginitis and mycotic vaginitis. The medicine composition provides a substantial effect in years of clinical applications.
US20110286926 Degradable hydrogel compositions and methods This invention concerns an in situ biodegradable hydrogel drug delivery system in which the components are assembled in a manner that provides a mechanism for the timed cleavage of a particular amide bond in a covalently linked active agent or of the hydrogel structure.
CN101514192B Quinoxalinone derivative with activity for reversing tumor cell multidrug resistance and preparation method thereof The invention discloses a quinoxalinone derivative with activity for reversing tumor cell multidrug resistance and a preparation method thereof, belonging to the technical field of pharmaceutical chemistry. The quinoxalinone derivative has a structure shown in the general formula (I), wherein, R1 and R2 are same or different and are respectively selected from C1-4 linear chain or branched alkyl, halogen, cyano-group, alkoxy group containing 1 to 4 carbon atoms and haloalkyl containing 1 to 4 carbon atoms; and R3 is selected from hydroxyl, methoxy, ethoxy, carboxyl methyl or ethyl substituted natural L-amino acid residue, optionally substituted other primary amine and optionally substituted secondary amine. A compound of the invention can increase the cell toxicant efficacy of K562/A02 multidrug resistance cell strain expressed by adriamycin towards P-glycosidoprotein in the experiment for screening the invitro pharmacological activity for reversing multidrug resistance cell strain K562/A02, and the quinoxalinone derivative is effective multidrug resistance reversal agent and is probable to be developed into novel chemotherapeutic drug sensitizing agent.
US7056895 1-(3,4-dihydroxy-5-methylol-tetrahydrofur-2-yl),3-amidino-1H-1,2,4- triazoles; infections, infestations, autoimmune diseases; anticarcinogenic and -tumor agents; HIV, hepatitis C, human papilloma virus and giant cell arteritis Novel heterocyclic aromatic compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.
US6844352 1′-[4-[1-(4-fluorophenyl)-1H-indole-3-yl]-1-butyl]-spiro[isobenzofuran-1(3H),4′-piperidine] hydrohalogenides The present invention relates to a hydrohalogenide of 1′-[4-[1-(4-fluorophenyl)-1H-indole-3-yl]-1-butyl]-spiro[isobenzofuran-1(3H),4′-piperidine], pharmaceutical compositions containing the acid addition salts and the use thereof for the treatment of psychic and neurological disorders.
CN101502502A Medicament composition for preventing and treating ischemia-reperfusion injury of kidney The invention relates to the application of iptakalim and the pharmaceutically acceptable salts thereof in the preparation of drugs for achieving the protective effect on renal ischemic reperfusion injury and controlling renal ischemic reperfusion injury and acute renal failure caused therefrom. The invention further relates to a drug combination for controlling the renal ischemic reperfusion injury, wherein, the drug combination comprises iptakalim or the pharmaceutically acceptable salts thereof, and at least one drug carrier or diluent.
US20110319355 Methods for treating non-small cell lung cancer using 5-azacytidine The present disclosure provides methods for treating subjects having non-small cell lung cancer, wherein the methods comprise administering to the subject a cytidine analog, such as 5-azacytidine. Also provided are methods relating to identification and treatment of particular non-small cell lung cancer types sensitive to particular cytidine analogs.
US20110003786 2-Carboxamide Cycloamino Ureas The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
US8673924 Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors In its many embodiments, the present invention provides a method of inhibiting one or more cyclin dependent kinases in a patient comprising administering to said patient a therapeutically effective amount of at least one pyrazolo[1,5-a]pyrimidine compound or a pharmaceutical composition comprising such compound, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. An example pyrazolo[1,5-a]pyrimidine compound useful in the present invention is shown below:
US20110207727 Thio-subsituted Anthra [1, 2-d] imidazole- 6, 11-dione Dervatives, Preparation Method and application thereof A series of novel thio-substituted anthra[1,2-d]imidazole-6,11-dione dervatives, and the preparation method and application of said derivatives, said application having a pharmaceutical composition containing said derivatives with therapeutically effective amount for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.
CN103479642A Nano sodium cantharidinate composition and preparation method thereof The invention relates to a nano sodium cantharidinate composition and a preparation method thereof. The composition comprises 0.1-30 parts of sodium cantharidinate, 0.1-15 parts of moroxydine, 10-50 parts of polyacrylic resin II, 10-40 parts of glyceryl monostearate, 95% of 300-500 parts of ethanol and 400-700 parts of water. The composition is prepared by a nanotechnology, the growth of hepatoma cells is well inhibited, and pain of patients is greatly relived; and formed micro-capsules are enteric, so that the sodium cantharidinate can be prevented from being reduced to cantharidin, and toxic and side effects are reduced.
CN102451413A Preparation method for sophora flavescens ointment The invention relates to a preparation method for a sophora flavescens ointment. The method comprises the following steps: immersing raw rhubarb, chaulmoogra, stemona, common cnidium fruit and divaricate saposhnikovia root with clear water, decocting the above mentioned materials in a boiler, filtering decoction, removing residues, concentrating the decoction until the decoction is five times that of the materials, grinding sulphur, alum and borneol into extremely fine powder, mixing the fine powder with an obtained concentrate to obtain a thick ointment, filling the thick ointment into a bottle and applying the ointment on a wounded part with a cotton swab during utilization. The ointment provided in the invention has the advantages of simple preparation, convenient usage and a good effect and is a good paste agent for treating acne rosacea.
CN101220000A Acyl chloride and sulfonyl chloride derivant, and uses thereof The invention belongs to an infection related medical field, providing acyl chloride and sulfonyl chloride ixazoline derivatives provided with structures of a general formula (I) and an acceptable salt for the derivatives in pharmacy: wherein, R1 in the formula equals to an aryl, which comprises C3-C6 heterocyclic radical of sulfur, oxygen and nitrogen atom, aryl and heterocyclic radical (comprising C3-C6 heterocyclic radical of sulfur, oxygen and nitrogen atom); the aryl singly or multiply substituted by halogen, oxhydryl, carboxyl, azyl, nitryl, nitrile grouping, C1-C6 alkoxy, C1-C6 dialkylamino, C3-C6 naphthene base, C3-C6 heterocyclic radical, aryl, substituted aryl and other radicals, comprises C3-C6 heterocyclic radical of sulfur, oxygen, nitrogen atom, aryl and heterocyclic radical (C3-C6 heterocyclic radical of sulfur, oxygen and nitrogen atom); wherein, the definitions of R2, R3, and R4 are the same as described in the specification. The invention further provides the compounds and the acceptable slat in pharmacy as medicines, in particular to the function as antibacterial medicines.
WO2009024889A3 Pharmaceutical composition comprising a hmg-coa reductase inhibitor and ezetimibe This invention relates to a pharmaceutical composition of a HMG-CoA reductase inhibitor and ezetimibe for oral administration comprising a first component comprising HMG-CoA reductase inhibitor or pharmaceutically acceptable salts thereof and an alkaline earth metal salt additive; and a second component comprising granules of ezetimibe. Further, it relates to a pharmaceutical composition for oral administration comprising ezetimibe and an alkaline earth metal salt additive.
EP1163528B1 Prediction of diabetes impaired wound healing Wound healing is impaired in many diabetics, who suffer increased risk of chronic foot ulceration and amputation. Diabetic patient with poor healing ability were found to possess significantly lower fasting urinary nitrate levels than diabetic patients with normal healing ability or non-diabetic controls, implicating decreased endogenous nitric oxide activity as the mediator of diabetes-impaired wound healing. Methods and kits are provided for predicting the wound healing ability of diabetic patients based on the levels of nitric oxide related products such as nitrate or nitrite in urine or other specimens. Methods are also provided for treating non-wound healing diabetics and monitoring diabetic ulcer treatment.
CN101095722A Eye drops and preparation method thereof The invention relates to a health liquid using plant materials as the main raw materials and its preparing process, wherein the liquid is prepared from butterflybush flower, cassia seed, wild chrysanthemum flower, Tribulus terrestris, Epuisetum hiemale, notopterygium root, bile of vertebrates, boneol, boracic acid, Ethylparabenum, borax, propylparaben and sodium chloride through steps of extracting, concentrating, alcohol depositing, water precipitating, decolorizing, diluting and filtering.
CN101073612A Externally-applied health-care product for relieving burn and scald and its production The invention is concerned with the method of preparation of the external health product for releasing burns and scald symptom that contents pearl 13.1%-18.0%, chrysanthemum 13.1%-18.0%, fresh orange peel 25.2%-32.4% and far infrared ceramics powder 3.4%-6.1%. The steps of preparation includes: removine the sundries of the raw materials, cleaning, drying, grinding, sieving, and mixing evenly, attempering to cream form by balsam. The medicine can promote the blood circulation around the burns and scald areas, dehydrate the necrotic tissues and detumescence to straighten the wound.
CN1771955A Soft capsule composition of compound cough-relieving and phlegm-eliminating medicine The present invention relates to medicine preparation, and is especially one kind of soft capsule of compound cough-relieving and phlegm-eliminating medicine. The soft capsule has medicine comprising guaifenesin 1 weight portions, dextromethorphan hydrobromide 0.01-0.5 weight portion, dispersing medium 1.2-5.0 weight portions, glycerin 0.05-1 weight portion, and surfactant 0.01-0.2 weight portion. It has high quality and is suitable for clinical application.
CA2707718A1 Abcg2 inhibitor The present invention relates to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The invention provides an acrylonitrile derivative represented by formula (1): (see formula 1) (wherein A represents an optionally substituted 3- to 8-membered heterocyclic ring) or a salt thereof.
CN1989956A Adapalene gel composition and its preparation The invention involves an Adapalene gel combination and its preparation method. The particle size of the disclosed Adapalene gel in the invention is small and the scope of it is below 100 mum, and it has better stability compared with ordinary agents. The preparation method includes: disintegrating the main drugs or disintegrating and sieving the main drugs and solid surface activator, adding them into solution of assisting solvent, finally pressing and sieving the prepared gel again, then producing the gel combination.
WO2011084366A2 Methods, compositions and drug delivery systems for intraocular delivery of sirna molecules Biocompatible intraocular drug delivery systems in the form of an implant for intraocular administration of siRNA molecules. The drug delivery systems may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy among others.
US20100168239 Use of Rasagiline for the Treatment of Multiple System Atrophy Disclosed is a method for the treatment of Multiple System Atrophy comprising administering to a subject an amount of R(+)-N-propargyl-1-aminoindan or a pharmaceutically acceptable salt thereof.
CN103751409A Externally applied medicine for high-temperature burn and application method thereof The invention discloses an externally applied medicine for high-temperature burn, which comprises the following raw materials: sargentodoxae caulis, daturae flos, rumex japonicus houtt, liquorices, spina gleditsiae, concha arcae, lysimachia capillipes hemsl, lysimachia foenum-graecum hance, cortex mori radicis, castor bean, halloysitum rubrum, szechuan lovage rhizome, radix angelicae, borneol, beewax, cinnabar, mastic and myrrh. The invention further discloses an application method for the externally applied medicine for high-temperature burn. The application method comprises the following steps: adding sesame oil and vaseline on the basis of all the raw materials to prepare unguent; or adding water for decocting and then adding a chlorhexidine acetate solution to prepare a spray preparation. The externally applied medicine for high-temperature burn has the functions of clearing away heat and toxic materials, diminishing inflammation, relieving pains, promoting blood circulation, removing blood stasis, removing slough, promoting growth of tissue regeneration, restraining skin ulcer and enhancing skin, and has rapid pain relieving and skin regeneration effect on the high-temperature burn such as the first degree burn, second degree burn, and third degree burn or a scald; when being used for treatment, the medicine is directly painted on a burned wound, is convenient to use and free from side effects; no pain is caused during the therapeutic process; the course of treatment is short; the recovery speed is high; the curative effect is significant.
WO2007036802A3 Sublingual dosage form comrising vitamin d analogue, in particular calcitriol Disclosed are pharmaceutical dosage forms of vitamin D analogues, such as calcitriol, methods for their preparation and uses.
CN102058550A Clopidogrel bisulfate tablet and preparation method thereof The invention relates to a clopidogrel bisulfate tablet and a preparation method thereof. Each clopidogrel bisulfate tablet comprises 25-75 mg of clopidogrel bisulfate measured in the term of clopidogre, fillers, disintegrants, solubilizers, flow aids and lubricants. In the invention, the method of adding granular microcrystalline cellulose and aerosil through airflow crushing disposal to a prescription is adopted, therefore, the process of dry granulating is simple and feasible, reproducibility is good, prepared products have high stability, and the requirement of continuous large-scale production can be satisfied.
EP1412362B1 THIENO¬2,3-d|PYRIMIDINEDIONES AS INHIBITORS OF T-CELLS PROLIFERATION The invention relates to a compound of formula (1)(A chemical formula should be inserted here - please see paper copy enclosed) wherein Q is -CO- or -C(R4)(R5)- (wherein R4 is a hydrogen atom or C¿1-4?alkyl and R?5¿ is a hydrogen atom or hydroxy group) and Ar is a 5- to 10-membered aromatic ring system wherein up to 4 ring atoms may be heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted by one or more substituents as defined in the specification. It also relates to methods of preparing, pharmaceutical compositions containing and methods of using the compound of the formula (1), particularly in the modulation of autoimmune disease.
US20110008306 Creatine-ligand compounds and methods of use thereof The present invention provides methods of treating creatine responsive states, such as a neurological disorder (i.e., Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis and creatine transporter defect) or a skin disorder, by administering a creatine-ligand compound, alone or in combination with an anti-inflammatory compound, to a subject.
CN102532148A Compound with anti-tumor effect in zephyranthes candida and separation preparation method and application thereof The invention discloses a compound with an anti-tumor effect in zephyranthes candida and a separation preparation method and application thereof, particularly discloses activity and a structure of an alkaloid compound derived from plant zephyranthes candida, and includes a separation, purification and preparation method and relevant activity of a compound N-phenethyl crinidine alkali, zephyranthes candida alkaline A and zephyranthes candida alkaline B, wherein the compound N-phenethyl crinidine alkali, zephyranthes candida alkali A and zephyranthes candida alkali B are good in anti-tumor activity. According to research proof, the compound has inhibitory activity on cell proliferation of tumor cells of leukemia HL-60 and K562, lung cancer A-549, liver cancer HepG2 and colon cancer HT-29 and can be used as medicine for curing tumor diseases such as leukemia, lung cancer, liver cancer, colon cancer.
CN101991484A Wound pain quick recovery application instrument The invention discloses a wound pain quick recovery application instrument, which comprises a body, a controller, a keyboard circuit, an indicator light, a display screen, and three current and voltage regulating circuits, wherein the controller is respectively connected with the keyboard circuit, the display screen, the three current and voltage regulating circuits, a timing circuit and the indicator light; and the output ends of the three current and voltage regulating circuits are respectively connected with three groups of positive and negative electrodes which are respectively connected to three groups of application metal sheets. The wound pain quick recovery application instrument has a reasonable structure, is convenient to use, can form an electric field on the wound surface, accelerates the quick healing of the wound surface, reduces scar tissues, alleviates pain, prevents fat liquoring and postoperative pulmonary embolism, and accelerates the recovery of myoneural junctions.
CA2812417A1 Cationic dry powders The invention relates to respirable dry particles that contain one or more divalent metal cations, such as calcium, in an amount of less than 3% by weight, and to dry powders that contain the respirable particles. The dry particles can further contain an active agent, or can be used as carrier particles to deliver an active agent.
US7670632 Saponin mixtures and compounds isolated from Acacia victoriae; glycosides of acacic or oleanolic acid; control of cell apoptosis and cytotoxicity; antitumor, -carcinogenic, -inflammatory and -proliferative agents; atherosclerosis The invention provides saponin mixtures and compounds which are isolated from the species Acacia victoriae and methods for their use. These compounds may contain a triterpene moiety, such as acacic or oleanolic acid, to which oligosaccharides and monoterpenoid moieties are attached. The mixtures and compounds have properties related to the regulation of apoptosis and cytotoxicity of cells and exhibit potent anti-tumor effects against a variety of tumor cells.
CN1634005A Clenbuterol hydrochloride plaster The disclosed lenbuterol hydrochloride plaster comprises a back lining layer for obstructing light rays, air and moisture, a medicament storage pressure-sensitive adhesive layer arranged on the back lining layer, high molecular polymer base material arranged in the medicinal pressure-sensitive adhesive layer, right amount of clenbuterol hydrochloride or its basic group, penetration accelerating agent, stabilizer, and adhesive agent, the medicinal pressure-sensitive adhesive layer surface is coated by an antiseizing protective coating layer.
US6869944 Method for treating a patient with neoplasia by treatment with a platinum coordination complex This invention provides a method for treating a patient with neoplasia by an adjuvant therapy that includes treatment with an antineoplastic platinum coordination complex.
CN1775215A Azasetron hydrochloride glucose injection formulation, and its preparing method and quality control technology The present invention discloses an antiemetic ayasetron hydrochloride glucose injection preparation, its preparation method and quality control technique. Its composition includes ayasetron hydrochloride 0.1g, glucose 40-50g and sodium hydrogen sulfite 0-20mg. All the above-mentioned components are added into injection water, and dissolved to 1000ml so as to obtain the invented product. Said preparation is a fluid infusion type preparation, and can be used for clinical application.
CN101428007A Process for producing diabecron sustained release tablet The invention relates to a preparation method for metformin hydrochloride sustained-release tablets. The preparation method comprises the following steps: firstly, dissolving ethyl cellulose into ethanol solution, blending the ethyl cellulose with metformin hydrochloride to produce granules, and drying and sieving the granules at 45 to 55 DEG C; secondly, dissolving hydroxypropyl methylcellulose into ethanol solution to produce bonding agent, blending the granules prepared in step one, hydroxypropyl methylcellulose, ethyl cellulose and pore forming agent, adding the bonding agent, performing sieving and granulation, adding hydroxypropyl methylcellulose and lubricant, evenly blending, detecting the content, determining the tablet weight, and pressing into plain tablets; thirdly, dissolving film forming agent, plasticizer, masking agent and glidant for hydroxypropyl methylcellulose and ethyl cellulose into ethanol solution, completely stirring for more than 1 hour to produce sustained-release preparation coating solution, and finally obtaining the metformin hydrochloride sustained-release tablets by performing film coating to the plain tablets. The sustained-release preparation not only embodies the main characteristics of the sustained-release preparation for continuous sustained release of drug, but also presents high bioavailability.
WO2013175508A3 Stable pharmaceutical composition of aripiprazole The present invention provides stable pharmaceutical composition of Aripiprazole. In one embodiment, the present invention encompasses the use of crospovidone having peroxide content of less than 80 ppm, advantageously less than 50 ppm, in a composition comprising aripiprazole, and eventually other suitable pharmaceutically acceptable excipient, to obtain a stable composition of aripiprazole. In another embodiment, the present invention provides a composition of aripiprazole, wherein the composition comprises aripiprazole, crospovidone having peroxide content of less than 80 ppm, advantageously less than 50 ppm, and eventually other suitable pharmaceutically acceptable excipient. In another embodiment, the present invention is directed to a stable composition of aripiprazole for use in the treatment of schizophrenia, bipolar disorder, and clinical depression.
US7304075 Aqueous solution of sitafloxacin and sodium chloride; photostable microorganisms A liquid preparation having improved light stability is provided, which comprises an aqueous solution containing sitafloxacin and sodium chloride.
WO2014152663A1 Crystalline forms of tyrosine kinase inhibitors and their salts The invention relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.
US20100028360 Methods for the modulation of brain progestagen signaling in the prevention and treatment of neurological disorders and neurodegenerative diseases The present invention relates to methods for modulating progestagen signaling for treating neurological disorders or neurodegenerative disease, or preventing or delaying its onset in individuals deemed by competent observation and testing to be susceptible thereto. Progestagens can be administered to elevate serum and brain levels of progestagens and induce neurogenesis. Progestagen therapy may prevent some of the neurodegenerative and cognitive changes associated with developmental and aging associated neurological disorders and neurodegenerative diseases. Progestagen therapy together with suppression of GnRH, kisspeptin, LH and/or FSH signaling also may be used for treating neurological disorders or neurodegenerative diseases. The invention also relates to methods for inhibiting or delaying blastulation during embryogenesis, and neurogenesis during embryogenesis, fetal, neonatal, childhood, puberty or adult life. Blocking progestagen, estrogen and/or opioid signaling with receptor antagonists will inhibit neurogenesis. The invention also relates to using progestagens in vitro to induce neurogenesis in embryonic or adult stem cells.
CN101011347A Slow release injection containing platinum compound and topoisomerase inhibitor Disclosed is a slow release injection containing platinum-group compounds and/or topoisomerase depressant, which comprises slow release microspheres and dissolvent, the slow release microspheres include platinum-group compounds selected from Nedaplatin, Capecittabine, Carboplatin, cisplatin, and/or topoisomerase depressant anticancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with PLA, Polifeprosan, PLGA and poly(dodecanedioic acid-tetradecanedioic acid), the topoisomerase depressant is selected from camptothecine, monohydric camptothecine, Topotecan, Lartotecan, Irinotecan, Etoposide or Teniposide. The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 60 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.
CN102232952A Photoaging inhibitor and skin thinning inhibitor The invention provides a new agent which is effective in inhibiting photoaging, especially inhibiting wrinkles generated by ultraviolet rays or skin thinning. The application of pyrro-quinoline quinine and/or salt allowed by the pharmacology of the pyrro-quinoline quinine in the preparation of the photoaging inhibitor is provided.
US20070065517 Modafinil Pharmaceutical Compositions Pharmaceutical compositions comprising modafinil in the form of particles of defined size and methods for preparing same. The particle size of modafinil can have a significant effect on the potency and safety profile of the drug.
CN102641237A Curcumin microemulsion ion sensitive in situ gel preparation for intranasal administration and preparation method thereof The invention discloses a curcumin microemulsion ion sensitive in situ gel preparation for intranasal administration, which uses curcumin as a raw medicine and adopts a surfactant, a cosurfactant, an oil phase and a gellan gum solution. According to the portions by weight, the preparation comprises 0.5-8 portions of curcumin, 4-25.6 portions of oil phase, 17-46.4 portions of surfactant, 17-46.4 portions of cosurfactant and 20-50 portions of gellan gum solution, wherein the mass concentration of the gellan gum solution is 0.1%-1.0%. The preparation method comprises the following steps of: firstly, uniformly mixing the oil phase, the surfactant and the cosurfactant in a mode of electromagnetic stirring, vortex oscillation or ultrasound; secondly, adding the curcumin, and fully stirring the mixture to be dissolved; thirdly, dropwise adding the gellan gum solution; and finally, continuously stirring the mixture to obtain the curcumin microemulsion ion sensitive in situ gel preparation for intranasal administration. After intranasal administration of the microemulsion ion sensitive in situ gel preparation disclosed by the invention, the medicine can reach brain targeted sites through a direct nose-brain path and a systemic circulation path, so that the curcumin has a treatment effect on brain tissues.
WO2007104897A1 Topical compositions in the form of an oil-in-water emulsion comprising a pro-penetrating glycol and a steroidal anti-inflammatory drug The invention relates to a novel composition in the form of an oil-in-water emulsion, for topical application, comprising a pro-penetrant system containing at least one glycol and at least one additional pro-penetrant agent, a suitable gelling agent, and at least one active substance of the group of steroidal anti-inflammatory drugs.
CN103655800A Medicine for treating prickly heat and preparation method thereof The invention discloses a medicine for treating prickly heat and a preparation method thereof. The medicine is mainly prepared from the following components at a certain weight ratio: gypsum rubrum, earthworm, peach leaf and lotus. The medicine has the effects of clearing away heat and toxic materials and dissipating heat and repelling foulness and is fast in effectiveness in treatment of prickly heat and is good in curative effect, and the prickly heat does not reoccur.
US20110033443 Method for Increasing Bone Mass The present invention features methods for promoting the differentiation of osteoblast bone forming cells to a mineralization phenotype and increasing bone mass using inhibitors of Brahma. Subjects benefiting from such treatment may have non-union fractures, osteopenia or osteoporosis, osteosarcoma, or a bone graft or bone fusion or orthopedic and dental implants, osteolytic bone disease, skeletal defects or deficiencies or periodontal disease.
CN1593431A Pharmaceutical composition for protecting liver The invention relates to a pharmaceutical composition for protecting liver, which is prepared from silymarin or extract of silymarin, phosphatides and medicinal auxiliary materials. The composition can increase the biological availability for silymarin.
CN101351446B Novel fused pyrrole derivatives The present invention is concerned with novel fused pyrrole derivatives of formula (I) wherein A, Ar, R<1>, R<2>, R<2'> and R<2''>and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.
WO2008009407A3 Sulphonylaminocarbonyl derivatives of bile acid amides for use as immunomodulators 4-(3-hydroxy-10,13-climethyl-hexaclecahyclro-cyclopenta[a]phenanthren-17-yl)-pentanoic acid amides wherein the nitrogen of the amide group is substituted by a sulfonylaminocarbonyl- (C14)-alkyl group; and the use of such compounds as pharmaceuticals.
US6979690 Oxo or oxy-pyridine compounds as 5-HT4 receptor modulators This invention provides compounds of the formula (I) and (II): or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R1 is hydrogen or halo; R2 and R3 are independently hydrogen or C1-6 alkyl; R4 and R5 are independently hydrogen or C1-6 alkyl; R6 is hydrogen, C1-12 alkyl, C1-6 alkoxy (C1-6)alkyl or C1-12 alkyl substituted by up to 3 substituents selected from the groups consisting of C3-8 cycloalkyl, aryl, heteroaryl and heterocyclic; R7 and R8 are hydrogen or taken together may form alkylene chain having one or two carbon atoms; R9 is C1-6 alkyl or C3-8 cycloalkyl; R10 is C1-6 alkyl or NR11R12; L is (CR11R12)n or NR11; M is NR11 or (CR11R12)n; R11 and R12 are independently hydrogen or C1-6 alkyl; n is an integer from 0 to 5; and m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and C1-6 alkyl; with the proviso that when R9 is C1-6 alkyl, L is not NR11. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
CN101235072A Oleanolic acid triterpene with A ring and C ring both containing multiple oxygen-containing substituents and use thereof The invention provides an oleanolic acid triterpenoid which A ring and C ring contain multiple oxygen substituents, represented as formula (1). The inventive compound can inhibit the growth activity of tumor cell to be applied in anti-tumor drug and can inhibit mice ear swelling caused by dimethylbenzene to be applied in anti-inflammatory agent. The formula (1) is represented as above.
US20120202758 Core 2glcnac-t inhibitors Treatments for conditions involving detrimental activity of the enzyme core 2 GlcNAc-T are provided using compounds of the formula I wherein R1 is H, —OH, C1-6 alkoxy, —NR5R6, or Sac 1; R2 is H, —OH, C1-6 alkoxy or Sac 2; R3 is H, —OH, C1-6 alkoxy or Sac 3; R4 is H, C1-6 alkyl, C1-6 hydroxyalkyl or C1-6-alkoxy-C1-6-alkyl; R5 is H, C1-6 alkyl or C1-6 acyl; R6 is H, C1-6 alkyl or C1-6 acyl; Sac 1 Sac 2 and Sac 3 are independently selected saccharide moieties; and Z is a steroid moiety; or a pharmaceutically acceptable salt, ether or ester form thereof
EP1631282A1 Use of the hydrochloride of the active ingredient base 1-[n2-[3,5-dibromo-n-[[4-(3,4-dihydro-2(1h)-oxoquinazolin-3-yl)-1-piperidinyl]-carbonyl]-d-tyrosyl]-l-lysyl]-4-(4-pyridinyl)-piperazine combined with sumatriptan for the treatment of migraines The invention relates to a method for the treatment or prevention of headaches, migraines or cluster headaches, said method including the combined administration of a therapeutically active quantity of the hydrochloride of the active ingredient base 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]-carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine (A) and a therapeutically active quantity of the migraine active ingredient sumatriptan or a physiologically compatible salt thereof. The invention also relates to the corresponding pharmaceutical compositions and to the production of the same.
US20100226977 Low viscosity phospholipid compositions The invention relates to processing crustaceans such as krill to oils comprising phospholipids that are Newtonian fluids and/or and have low viscosity, and in particular to the production of oils containing astaxanthin and phospholipids that show Newtonian fluidity and have a low viscosity.
CN103044449A Novel ceftizoxime sodium compound and medicine composition thereof The invention discloses a novel ceftizoxime sodium compound, which has the purity greater than 99.5%. The invention further discloses a medicine composition of the ceftizoxime sodium compound. The medicine composition comprises the following components in part by weight: 20 to 90 parts of ceftizoxime sodium, 3 to 9 parts of glycine, 5 to 12 parts of methionine, 2 to 5 parts of sorbitol, and 1 to 3 parts of sodium hydrogen sulfite. When the novel ceftizoxime sodium compound is used in combination with glycine, methionine, sorbitol and sodium hydrogen sulfite, glycine and methionine can work together to greatly improve the stability of the ceftizoxime sodium medicine composition.
CN102147360A Detection method for drug combination The invention discloses a method for detecting the content of acetaminophen and moisture in a drug combination (999 Ganmaoling particles) for treating influenza by using near infrared spectrums; a corresponding acetaminophen content model and a corresponding water content model are established; a chemical method proves that the deviation of cross validation is very small; and the invention confirms that the method for determining the content of components in the drug combination (999 Ganmaoling particles) by adopting a near infrared spectrometer and configuring an integrating sphere diffuse reflection module is achievable.
US20080214508 O-phosphonooxymethyl propofol disodium salt; anasthetic, analgesic, anxiolytic agent, antidepressant; bioavailable and pharmacologically active when given by intravenous, than subcutaneous or rectal administration A method of administering a prodrug of propofol, preferably O-phosphonooxymethyl propofol disodium salt, comprises the subcutaneous or rectal administration of the prodrug in amounts sufficient to induce or maintain a generalized anesthetized state, a conscious sedated state, or to treat insomnia, anxiety, nausea, vomiting, pruritus, epilepsy, and a range of pain syndromes, including migraine pain, and other medical conditions.
WO2014013025A1 Baclofen and acamprosate based therapy of macular degeneration disorders The present invention relates to combinations and methods for the treatment of macular degeneration disorders. More specifically, the present invention relates to novel combinatorial therapies of Age related Macular Degeneration based on baclofen and acamprosate combination.
EP1633369B1 Process to minimize loss through adhesion to equipment surfaces The invention relates to a new process for preparing combination formulations of inhaled glucocorticoids and beta 2-agonists, e.g. budesonide in combination with formoterol. The process aims at minimizing adhesion of one or more of the ingredients to equipment surfaces by adding the ingredients to a container in a stepwise manner.
WO2010075636A1 Compounds and methods for treatment of influenza The present invention provides in part a compound of Formula (I) or a pharmaceutically- acceptable salt or stereoisomer thereof: where R1 is selected from the group consisting of a substituted triazole group, a guanidine group, a urea group, a thiourea group, an amidine group, and N3; and R2 is selected from the group consisting of H, Me, Et and an amino acid, and methods and uses thereof.
WO2013135745A1 Methods of treating melanoma with pak1 inhibitors The present invention provides methods and compositions for the treatment of melanoma using a PAK1 inhibitor. In some embodiments, PAK1 is overexpressed and/or amplified in the melanoma. In some embodiments, the melanoma is a wild-type BRAF melanoma.
CN101884625A Berberine tannate dispersible tablet and preparation method thereof The invention provides an antibacterial agent berberine tannate dispersible tablet and a preparation method thereof. The formula comprises berberine tannate as the principal agent and auxiliary additives, wherein the auxiliary additives are the additives of the common dispersible tablet preparation, and a flavoring agent is added. A full-powder direct tablet compressing method or a tablet compressing wet granulation method can be adopted, and the tablet can be a plain tablet or a film-coated tablet. Compared with other preparations, the invention has the characteristics of rapid disintegration, quick dissolving out and good disperse state. Based on the berberine tannate tablet for children, the invention provides the dispersible tablet which is prepared by changing the preparation and can be taken by children conveniently, and the dispersible tablet can rapidly disintegrate in saliva and be dissolved into a sweet liquid medicine, thus the dispersible tablet is taken by keeping in mouth and sucking, can be accepted and taken more easily by children, and has convenient use.
CN101090896B Novel benzo-fused heteroaryl sulfamide derivatives useful as anticonvulsant agents The present invention is directed to novel benzo-fused heteroaryl sulfamide derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.
CN101348511A Synthesis and refinement of nelarabine The invention discloses a method for preparing and refining a nucleotide compound, and particularly a method for preparing and refining Nalarabine. The preparation method has low requirements on facilities, with shorter synthesis process and simplified operation; the yielding rate of the whole production line is high with low production cost, and the method is economically viable and suitable for industrialized production. In addition, the invention also discloses a method for synthesizing an intermediate of Nalarabine.
CN102875633A Betulonic acid ester derivative and preparation method and application thereof The invention discloses betulonic acid ester derivative and a preparation method and application thereof. Compound structure of the betulonic acid ester derivative is shown in a formula (I) and a formula (II). The betulonic acid ester derivative is synthesized with betulonic acid, halogenated hydrocarbon, secondary amine, piperazine, aromatic acid and replacement aromatic acid by substitution reaction and acid-amine condensation. The betulonic acid ester derivative can be used to prepare anti-cancer drugs.
CN102525900A Levetiracetam injection and preparation method thereof The invention designs a prescription of a levetiracetam injection and a preparation method thereof. The prescription is mainly composed of levetiracetam as an active component as well as an acetate buffer solution, sodium chloride and water for injection. The preparation method of the prescription comprises the steps of: weighing the components, stirring for dissolving, adding 0.05%-0.2%(W/V) activated carbon for injection, performing pressure filtration on the liquor to remove pyrogen, regulating the pH value of the solution to be in a range of 5.0-6.0, performing coarse filtration with a 0.45mu m filter membrane, then performing fine filtration with a 0.22mu m filter membrane, filling into 5ml penicillin bottles after quality inspection pass, capping and sealing, and sterilizing under a terminal sterilizing condition of 121 DEG C for 15 minutes. The levetiracetam injection produced by the invention has a high sterility level, and the safety performance is more fully guaranteed for clinical medication.
WO2011006638A1 Process for the synthesis of paliperidone The invention describes an improved process for the synthesis and purification of paliperidone.
CN101057856A Fast recovery agent for seeding vitality used in aquiculture The invention relates to a fast recovery agent for aquaculture, which is used to recover seed activity and increase seed survival rate, belonging to the field of aquaculture technique. It mainly takes glucose, taurine, inosine, vitamin C, vitamin B1, and vitamin B2. The method for preparing recovery agent comprises: weighing raw material according to proportion, mixing at room temperature and packing. The invention will generate no stimulation to seed, the water solubility of recovery agent is good and can be immersed for absorption, it can improve fatigue condition after long transportation, enhance adaptability to new pool environment, and increase seed survival rate.
DE102009056597A1 Use of flavin derivatives and their salts for preparing a medicament for the treatment of pathologies of the internal limiting membrane (ILM), and the flavin derivative is riboflavin or roseoflavin Use of flavin derivatives and their salts for preparing a medicament for the treatment of pathologies of the internal limiting membrane (ILM), is claimed. The flavin derivative is riboflavin or roseoflavin, which can be photodynamically degraded by a irradiation from an intra- or extravitreal light source with a wavelength of 500 nm and an effective intensity of 5 mW/cm 2>, after an intravitreal application of the ILM. The ILM or the its adjacent structures are generated by a mechanical stabilization. - ACTIVITY : Ophthalmological. Test details are described but no results given. - MECHANISM OF ACTION : None given.
US20060013801 Prevention of and therapy for radiation toxicity of normal tissues using drugs which block il-1 activity A method for the prevention of and therapy for radiation pneumonitis, dermatitis, soft tissue fibrosis and central nervous system toxicity in patients undergoing therapeutic radiation. In addition, the invention provides for pre-treatment of those responding to nuclear bio terrorism or other nuclear or radiological accidents. Thus, with the present invention, subjects may be treated in order to prevent toxicity from nuclear bio terrorism or other nuclear or radiological accidents. More particularly, we have discovered a method for prophylactically treating radiation toxicity in normal tissue of subject comprising administering an anti-radiation toxicity effective amount of a cytokine blocking agent through the subject. More specifically, we have discovered a method for prophylactically treating radiation pneumonitis, dermatitis, soft tissue fibrosis or central nervous system toxicity in a subject comprising administering an anti-radiation pneumonitis, dermatitis, soft tissue fibrosis or central nervous system toxicity effective amount of a cytokine blocking agent to the subject.
CN102114216A Externally applied antibacterial and antiphlogistic medicament and preparation method thereof The invention discloses an externally applied antibacterial and antiphlogistic medicament and a preparation method thereof, and relates to an antiphlogistic medicament and the preparation method thereof. The antiphlogistic medicament is processed and prepared by the following raw materials: peppermint, fineleaf schizonepeta herb, divaricate saposhnikovia root, rhubarb, amur corktree bark, common andrographis herb, fructus forsythiae, baical skullcap root, Philippine violet herb, radix salviae miltiorrhizae, lightyellow sophora root, dahurian angelica root, tree peony bark, aloe, membranous milkvetch root, indigowoad leaf, sweet wormwood herb, Chinese gentian, sinkiang arnebia root, liquoric root, Chinese gall, golden thread, cassia seed, indigowoad root, honeysuckle flower, chrysanthemum, hawthorn fruit, sessile stemona root, argy wormwood leaf, common cnidium fruit, borneol powder, borax powder, honey, propanetriol, propanediol, Tween-60, OP10, castor oil and turpentine oil. The product has good antibacterial and antiphlogistic effects, bacteria can not generate an antibody and can not generate the resistance to the medicament, the bacteria can be prevented from being mutated to superbacteria, and the antiphlogistic medicament has no toxicity or side effects and is safe to use.
CN101244027A Artemether percutaneous drug administration preparation for treating dermatosis The invention relates to a transdermal drug delivery system of artemether, which comprises artemether of main drug, transdermal absorption enhancer or percutaneous absorption carrier and other pharmaceutical adjuvant. Antimalarial artemether can be used as a new immunomodulator and can be used for treating certain skin disease through study showing. The artemether of the transdermal drug delivery system can directly act on skin surface of patients and enter dermis layer and subcutaneous tissue through penetrating through epidermis. The transdermal drug delivery system of artemether can greatly increase dosage of artemether in skin of patients to increase therapeutic effect at lower dosage compared with other drug delivery mode of artemether. The transdermal drug delivery system of artemether has the advantages of convenient drug delivery, strong targeting, no skin irritation and simple preparation. The transdermal drug delivery system of artemether can be used for treating skin diseases such as polymorphous light eruption, vegetable-solar dermatitis, atopic dermatitis and eczema.
WO2007098680A1 The uses of d-limonene, plant or valatile oil thereof containing d-limonene in manufacturing medicaments for preventing and treating diabetes The uses of d-limonene, plant or volatile oil thereof containing d-limonene in manufacturing medicaments for preventing and treating diabetes.
US20110166207 Use of aav integration efficiency element for mediating site-specific integration of a transcription unit The invention provides an expression construct comprising a nucleic acid sequence encoding an adeno-associated virus integration efficiency element (AAV IEE), wherein the expression construct is substantially devoid of AAV inverted terminal repeats (AAV ITRs). Such an expression construct site-specifically integrates into a host cell chromosome when provided to a host cell in conjunction with an AAV Rep protein. The invention also provides a method of integrating a nucleic acid sequence of interest into a host cell chromosome through use of such an expression construct, as well as a method of prophylactically or therapeutically treating a mammal for a pathologic state comprising administering to a mammal such an expression construct comprising a nucleic acid sequence encoding a therapeutic factor.
WO2013073576A1 Nucleic acid molecule for inhibiting activity of rnai molecule The purpose of the present invention is to develop and provide a nucleic acid molecule which can inhibit the activity of an target RNAi molecule specifically and with high efficiency and can be produced safely at low cost. Provided is a nucleic acid molecule for inhibiting the activity of a target RNAi molecule, comprising: a single-stranded nucleic acid moiety which contains one un-modified DNA region comprising a nucleotide sequence completely or satisfactorily complementary to a nucleotide sequence for a functional chain that is contained in the target RNAi molecule and has the activity; and a double-stranded nucleic acid moiety which is connected to the 5'-terminal and/or the 3'-terminal of the single-stranded nucleic acid moiety.
US7491707 Synthetic lipid-a-analogs and uses thereof New synthetic Lipid-A analogs based on monosaccharide (1) and disaccharide (2) derivatives were designed and prepared in the present invention. Both structures (1) and (2) incorporate novel lipid structures (3) and (4) that are not found in nature. Also, novel disaccharide Lipid-A structures (2) that incorporate novel contingents of uniform lipids and where R1, R4 and R5 are the same substitution group of structure (III) were synthesized. Liposome formulations containing totally synthetic components such as synthetic Lipid-A and synthetic lipopeptide derived from tumor-associated MUC1 mucin are described along with their therapeutic utility. Comparative test results of immunostimulating properties and toxicity of Lipid-A analogs (1) and (2) are included.
US20110124683 Use of CRTH2 Antagonist Compounds The invention relates to compounds of general formula (I): wherein R1, R2, R3, R4 and R5 are as defined herein for the treatment of allergic conditions, wherein the treatment is by pulsed therapy which comprises a first period during which the compound is administered to the patient and a second period of at least seven days during which the compound is administered to the patient in a reduced amount. The invention also relates to compounds of general formula (I) for desensitizing the immune system of a subject to allergens, thus preventing or reducing the symptoms of allergic conditions such as allergic asthma, allergic rhinitis, or atopic dermatitis.
US7186751 anticarcinogenic agents comprising a mixture of taxol, solubilizers, stabilizers and anhydrous ethanol, having superior solubility, stability, bioavailability and side effect reduction The disclosure concerns an injectable composition of paclitaxel, more particularly, an injectable composition of paclitaxel having excellent anticancer effect comprising solubilizer such as polyoxyl hydrogenated castor oil, anhydrous ethanol and stabilizer such as N-acetyl amino acid. The injectable compositions of paclitaxel provide a medical effect higher than that of the known compositions showing not only a lower toxicity but also superior solubility of paclitaxel and stability at room temperature, thus enabling venous injection by having fine particles.
CN101969939A Alpha adrenergic receptor agonists for treatment of inflammatory diseases Effective treatments of pain and/or inflammation from tendonitis, carpal tunnel syndrome, tarsal tunnel syndrome, osteoarthritis, bursitis and/or an oral-facial disease are provided. Through the administration of an effective amount of at least one alpha adrenergic agonist at or near a target site, one can reduce, prevent or treat pain and/or inflammation from tendonitis, carpal tunnel syndrome, tarsal tunnel syndrome, osteoarthritis, bursitis and/or an oral-facial disease.
CN101822693A Medicine treating tympanitis The invention provides a medicine treating tympanitis, which comprises 100g fresh eel blood, 10g earthworm dried powder, 5g musk dried powder, 2g toadfish dried powder and 50g French chalk. When used to treat tympanitis, the invention has the effects of quick curative effect, stopping pain, clearing heat and toxic material, eliminating putridity and engendering the new, good curative effect, short treatment period, convenient use and security. The invention is applicable to the clinical treatment of tympanitis.
CA2239582C A new therapeutic use for glycine Glycine is indicated to prevent or treat acute or chronic graft rejection, optionally in combination with an immunosuppressant or an immunomodulating agent.
CN103432086A Pemetrexed disodium freeze-dried powder injection for injection and preparation method thereof The invention discloses a pemetrexed disodium freeze-dried powder injection for injection and a preparation method thereof. The pemetrexed disodium freeze-dried powder injection contains disodium hydrogen phosphate and dipotassium hydrogen phosphate buffer salt, wherein the weight ratio of disodium hydrogen phosphate to dipotassium hydrogen phosphate is (8-10):1, and the pH value of liquid medicine is 6.5-7.5 before freeze-drying. The pemetrexed disodium freeze-dried powder injection disclosed by the invention enhances the pharmaceutical stability, has the advantages of less auxiliary material variety and usage amount, more safety and reliability and simple preparation process, and meets the requirement for mass production.
CN1931214B Medicine composition of rhodiola root and puerarin The present invention belongs to the field of medicine technology, and is especially one kind of medicine composition for treating cardiac and cerebral vascular diseases and its preparations and preparation process. The medicine composition consists of rhodiola root in 300-1800 weight portions, preferably 1000 weight portions, or its extract, and puerarin in 30-500 weight portions, preferably150 weight portions. The composition may be prepared into different pharmaceutically acceptable forms, preferably injection. The composition has synergistic effect and high stability.
CN101322802A Paste for curing psoriasis and preparation thereof The invention discloses an external paste for treating psoriasis. The external paste consists of the following raw materials with the weight proportion by parts: 16-22 parts of pot soot, 8-15 parts of manyflower wormwood herb, 1-5 parts of natural indigo, 4-8 parts of calcined horse lizard, 4-8 parts of calcined gypsum, 2-5 parts of chaulmoogratree, 1-3 parts of realgar, 4-6 parts of calomel, 10-14 parts of phellodendron bark, 4-8 parts of colophony, 1-3 parts of sulfur, 2-6 parts of unbracteolated spurge root, 2-6 parts of Chinese ephedra, 1-3 parts of serrate chloranthus root and 1-3 parts of cochinchina momordica seed. All the raw materials are ground into fine powder, the fine powder is poured into and evenly mixed with 500 parts of soot, and then the mixture is soaked for 40 to 60 days, thus the external paste is obtained. The external paste of the invention has the advantages of high curative ratio, no relapse after healing and low treatment cost.
US20050123593 Chondroitin sulfate, keratinsulphate, heparin, heparin sulfate and dermatan sulfate encapsulated in a bilayer forming dipalmitoylphosphatidylcholine phospholipid; dosage; osteoarthritis In a preferred embodiemnt the present invention features a composition and method of delivery comprising Glycosaminoglycans encapsulated in a liposomal delivery system for intraarticular administration for the treatment of osteoarthritis In a more preferred embodiemnt the present invention features a composition and method of delivery comprising hyaluronic acid encapsulated in a liposomal delivery system for intraarticular administration for the treatment of osteoarthritis.
CA2408887C Medical composition kit for treating lesioned abnormal tissue Optimum compounding composition of a local injection preparation for treating rectal submucous lesioned abnormal tissue with local anesthetic is decided to provide a medical composition kit. In a composition kit for the treatment where respective containers are unsealed upon being used and respective contents are mixed to obtain a preparation for injection, a medical composition kit which is characterized in that respective single doses of a therapeutic preparation and local anesthetic are fractionally charged in containers, the said therapeutic preparation contains 1-10% of a water-soluble aluminum compound and 0.01.THorizBrace.2% of tannic acid and the said local anesthetic contains 0.1.THorizBrace.1% of lidocaine hydrochloride or 0.5-5% of procaine hydrochloride.
CA2578231A1 Sulpiride derivatives pharmaceutical compositions The present invention relates to pharmaceutical compositions containing sulpiride compounds having the general formula (I): where R1 is branched or straight chain alkyl having from 1 to about 7 carbon atoms, a substituted or unsubstituted aryl, a substituted or unsubstituted cycloalkyl, a substituted or unsubstituted aralkyl, a substituted or unsubstituted alkylcycloakyl, or a group having the formula (CH2)n R2 where R2 is a substituted or unsubstituted aryl or a substituted or unsubstituted cycloalkyl, and n is an alkyl group having from 0 to about 6 carbon atoms and pharmaceutically acceptable salts or diluents.
WO2006043783A1 Pharmaceutical compositions, comprising red ginseng acid polysaccharide and lentinus edodes, of preventing and treating cancer This invention relates to a pharmaceutical composition which is useful for the treatment of tumors, comprising RGAP and Lentinus edodes extract as active ingredients, wherein its selective augmentation on the level of immunoglobulin IgM may lead to rapid recovery of immunity in the body, thus promoting longevity and maximizing antitumor activity.
CA2559237A1 Novel alkyne compounds having an mch-antagonistic effect and medicaments containing said compounds The invention relates to alkyne compounds of general formula (I), in which groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings cited in Claim 1. The invention also relates to medicaments containing at least one inventive alkyne. The MCH receptor antagonistic effect renders the inventive medicaments suitable for treating metabolic disorders and/or eating disorders, in particular, obesity and diabetes.
US6855520 Cell volume-regulated human kinase h-sgk The present invention relates to the cloning and characterization of a human serine/threonine kinase (h-sgk: serum and glucocorticoid dependent kinase). The invention furthermore relates to reagents for diagnosing conditions associated with a change in cell volume and/or in “macromolecular crowding” in the body, such as, for example, hypernatremia, hyponatremia, diabetes mellitus, renal failure, hypercatabolism, hepatic encephalopathy, inflammation and microbial or viral infections. The present invention additionally relates to pharmaceuticals comprising the h-sgk, nucleic acids which code for the h-sgk, or receptors, in particular antibodies, which specifically bind to the h-sgk.
WO2005112881A8 The dispersible montmorillonite tablet and its preparation technology A dispersible montmorillonite tablet and its preparation technology as well as the new pharmaceutical formulation which consists of montmorillonite, fillers and disintegrant and is characterised by the stability of qulity, quickly disintegrating and homogeneous dispersing, easy dose controllability, flavoured taste, smooth surface of the tablet and the homogeneous colour as well.
US20080181946 Controlled Release Delivery System For Metformin The invention relates to a controlled release delivery system for Metformin comprising of (a) therapeutically effective amount of Metformin or pharmaceutically acceptable salts there of; (b) hydrophilic polymers and (c) hydrophobic lubricating agent(s). The invention also relates to a method of making the said solid dosage form.
CN1857440A Preparation and application of total paeoniflorin composition The present invention relates to compound preparation with general peony glycoside composition as main component for treating cardiac and cerebral vascular diseases. The general peony glycoside composition contains general peony glycoside in 1-99 wt%, and sowthistle-leaf ixeris flavonid and saponin, or seabuckthorn flavonid in 1-99 wt%, and is compounded with pharmaceutically acceptable supplementary material to prepare pharmaceutically acceptable preparations. The medicine of the present invention is used in preventing and treating cardiac and cerebral vascular diseases, senile dementia, and other diseases.
CN103288745A 2,6-disubstituted pyridazinone compound and application thereof The invention relates to a 2,6-disubstituted pyridazinone compound. The chemical structural formula of the compound is as shown as in the following formula (I). The compound provided by the invention can be obtained by reacting 6-(2-methoxyphenylethylamino)-3-(2H)-pyridazinone with 1-(3-bromopropane)-4-(2-chlorphenyl) piperazine. The 2,6-disubstituted pyridazinone compound provided by the invention has the advantage that an effect of inhibiting alpha 1-adrenergic receptors is obviously enhanced.
CN103751139A Lurasidone orally disintegrating tablet The invention belongs to the field of pharmaceutical preparations and in particular relates to an orally disintegrating tablet containing lurasidone or a salt thereof and a preparation method thereof. The orally disintegrating tablet is a pharmaceutical composition containing the lurasidone or a pharmaceutically acceptable lurasidone acid addition salt and amorphous silicon dioxide, wherein the particle size range of the lurasidone or the salt thereof is 0.1-10 mu m, the using amount of the amorphous silicon dioxide is 1-30%, and the orally disintegrating tablet has effective storage life. The invention provides the lurasidone orally disintegrating tablet with convenient preparation process, low production cost and effective storage life and aims at providing the preparation containing the lurasidone or the pharmaceutical acceptable salt thereof, which has the advantages of convenience in administration, rapidness in absorption and high bioavailability, for patients.
CN103230383A Calcium dobesilate capsule composition and preparation method thereof The invention belongs to the technical field of medicines, and concretely discloses a calcium dobesilate capsule composition and a preparation method. Calcium dobesilate is used as a raw material, and the composition also comprises one or a plurality of pharmaceutically acceptable excipients. The preparation method of the composition comprises the following steps: mixing calcium dobesilate with magnesium stearate to obtain a mixture, mixing the mixture with a selectable diluent, adding a proper amount of an adhesive to prepare a soft material, sieving to prepare wet particles, drying the wet particles, sieving for granulation, adding a corresponding lubricant, mixing, and filling to a capsule. The composition has the advantages of simple preparation method, consistency of a dissolution curve with that of reference listed drugs, and guarantee of the effective plasma concentration and the safety. The composition can be used for the diabetic microangiopathy.
WO2011147280A1 Injection of enrofloxacin and producing method thereof An injection of enrofloxacin and the producing method thereof are disclosed. The injection comprises from 10 to 20 parts of enrofloxacin, from 0.1 to 0.5 part of antioxidant and from 0.1 to 0.5 part of chelating agent and has a neutral pH value. The antioxidant is sodium bisulfite or sodium thiosulfate. The chelating agent is EDTA. The injection is stable and not irritative. Its producing method comprises the steps of: (1) adding enrofloxacin to the aqueous solution of sodium hydroxide; (2) continuing adding the aqueous solution of sodium hydroxide to obtain a pH value of 9-13; (3) adding acidifying agent to obtain a neutral pH value; (4) adding the antioxidant; (5) adding the chelating agent; (6) adding water to obtain the final product. The acidifying agent in step (3) is one or two or three selected from the group of lactic acid, sodium butyrate and arginine.
WO2010081851A1 Piperidin-4-ylpiperazine compounds for the treatment of hcv infection The invention relates to new piperazine-pieridine compounds having anti-viral activity and particularly anti-HCV activity. The invention further relates to pharmaceutical compositions comprising compounds according to the invention.
US20100256079 Eriocitrin-containing material, method for production of the eriocitrin-containing material, and food, beverage, pharmaceutical preparation and cosmetic each comprising the erocitrin-containing material A process for producing an eriocitrin-containing material comprises the steps of: preparing an eriocitrin-containing citrus extract from a citrus fruit using an extractant; and separating eriocitrin from the citrus extract. The step of separating eriocitrin from the citrus extract comprises the steps of: bringing the citrus extract into contact with a porous synthetic adsorption resin such that eriocitrin in the citrus extract is adsorbed on the porous synthetic adsorption resin, the porous synthetic adsorption resin comprising a phenol-formaldehyde resin as a main framework and having amino and phenolic hydroxyl groups; and eluting the eriocitrin adsorbed on the porous synthetic adsorption resin using an elution solvent.
CN101229158B Medicine compounds for treating tumour and applications thereof The invention discloses a drug composition and the application of the drug composition which is used for curing tumors, comprises anti-tumor active substances such as rapamycin (rapamycin) or derivatives and oridonin or acanthopanax and can be prepared into oral solid preparations and injections; wherein, a solid preparation unit comprises a kernel and an external drug layer, and the kernel comprises the oridonin or acanthopanax, and the external drug layer comprises a drug composition of the rapamycin and paclitaxel; the injections comprising the drug composition comprise the rapamycin with the concentration of 1 to 30mg/ml, the oridonin with the concentration of 5 to 300mg/ml or mixed solution of water diluents and solution of the drug composition of the acanthopanax and the paclitaxel with the concentration of 0 to 50mg/ml in propylene glycol. The invention can achieve good treatment effects through the synergistic effect of the anti-tumor active substances.
CN101897695A Medicinal preparation for treating prostatitis The invention discloses a medicinal preparation for treating prostatitis, and the active ingredient of a natural medicament and a preparation method thereof. The medicinal preparation is characterized by comprising 90 to 97 percent of psoralen, wherein the psoralen contains two impurities, namely 3 to 8 percent of corylifolinin and less than 1 percent of bakuchiol; preferably, the medicinal preparation comprises 95 to 97 percent of psoralen, and the psoralen contains 3 to 4.5 percent of corylifolinin and less than 0.5 percent of bakuchiol; and more preferably, the medicinal preparation comprises 96 to 97 percent of psoralen, and the psoralen contains 3 to 4 percent of corylifolinin and less than 0.1 percent of bakuchiol. Pharmacodynamic experiments prove that the active ingredient has good effect of treating male erectile disorder.
EP1694667A2 Polymorphs of 1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3, 3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid hydrochloride and mesalyte salts A polymorphic forms of the hydrochloride salt and mesylate salt of racemic (±)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid, dextrorotatory R-(+)-1-cyclopropyl-ó-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid and S-(-)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid having formula (I) and (II) respectively are described. Processes for their preparation are also described. The invention further relates to methods of using, and pharmaceutical compositions comprising the compounds of the invention for treatment of bacterial infections in mammals.
CN1973831A Magnetic slow releasing diclofenac sodium prepn in supermolecular intercalation structure and its prepn The present invention is magnetic slow releasing diclofenac sodium in supermolecular intercalation structure and its preparation process, and belongs to the field of hydrotalcite material technology. The magnetic diclofenac sodium has the chemical expression of (M2+)1-x(N3+)x(OH)2(DIK-)a(Bn-)b.mH2O.kM'Fe2O4, and is prepared through the first coprecipitation process to prepare nanometer magnetic kernel, the subsequent mixing of the magnetic kernel with corresponding salt solution, and the final coprecipitation process to assemble diclofenac sodium into the hydrotalcite layers and to obtain the diclofenac sodium intercalated hydrotalcite with magnetic kernel. The magnetic slow releasing diclofenac sodium in supermolecular intercalation structure has high stability, raised bioavailability, capable of magnetic field location and targeting location and effective control on the medicine structure, composition, etc.
CN103479732A Oral liquid for treating dog influenza and preparation method thereof The invention discloses oral liquid for treating dog influenza and a preparation method thereof. Every 100 liters of the oral liquid comprises the following materials by weight: 25-40 kilograms of radix astragali, 30-45 kilograms of honeysuckle flowers, 70-80 kilograms of fructus forsythiae, 1.5 kilograms of baicalin, 15 liters of dimethyl acetamide, 5-15 kilograms of acetaminophen and the balance of purified water. The oral liquid for treating the dog influenza, which is disclosed by the invention, is a compound preparation, adopts a Chinese and western medicine compound preparation, has the effect of clearing away heat and toxic materials through the honeysuckle flowers, the fructus forsythiae and the baicalin, has the effects of fast bringing down a fever and diminishing inflammations through the acetaminophen, has the effects of tonifying qi and elevating Yang through the radix astragali, can enhance the resistance of an organism, has the effects of resisting viruses, fast bringing down the fever and diminishing the inflammations, enhancing the resistance of the organism, preventing secondary infection and treating both symptoms and root causes on the dog influenza by jointly using medicines, is favorable to fast rehabilitation of diseases, plays a health restoration role, is favorable to reducing the suffering of an ill dog and can be used for treating both symptoms and root causes.
CN101152207A Application of laver polyoses in preparing medicament for preventing and treating neurous system disease The invention provides a laver polysaccharide which has the purpose of preventing and treating nervous system diseases. The invention is highly safe and can be taken for a long term.
CN202236430U Medicinal patch for treating onychomycosis The utility model discloses a medicinal patch for treating onychomycosis, aims at overcoming the defects in the prior art, and provides a novel medicine for treating the onychomycosis. The medicinal patch is divided into two parts. A first part is a nail dissolving patch (1); the nail dissolving patch mainly comprises five main structures and consists of a medical thermal pressure-sensitive adhesive (2) as shown in an attached drawing 1 in the specification, PC (polycarbonate) foam cotton (3), a silicon gel mat (4), spunlaced plain cloth (5) as shown in an attached drawing 2 in the specification, and blue mono-silicon glassine paper (6); a second part is nail dissolving paste (7); and the nail dissolving paste is made by mixing medicines of trichlorine-2, hydroxy diphenyl ether, medical petroleum jelly and the like. The defect that the medicines cannot be enabled to directly aim at the cause of a disease by soaking an ill nail with the medicines or coating the ill nail with the medicines conventionally is broken; aiming at the cause of the disease of the onychomycosis, the treatment is carried out in a targeted way; and by using the medicinal patch for treating the onychomycosis, a solution cavity of about 0.5 centimeter can be enabled to appear on the ill nail through the pharmacological actions of the medicinal patch, so that the medicines can reach a nail bed through the solution cavity, thereby killing germs on the nail bed and repairing the damaged nail bed.
CA2326517C New galenic preparations of meloxicam for oral administration The invention relates to the use of a meloxicam salt of an inorganic or organic base for preparing an orally administered, solid pharmaceutical preparation from which the active substance is rapidly released and absorbed, for pain therapy, corresponding pharmaceutical preparations made by direct tabletting and the process for preparing them.
CN101103980A Fexofenadine medicinal composition The invention relates to a pharmaceutical compound of Fexofenadine, containing Fexofenadine and excipient acceptable in at least one drug.
CN1778201A Composition with blue aeterio, grape seed and cassia seed A composition for preparing the food and medicine to prevent and treat ophthalmopathy caused by eye fatigue is prepared from blueberry fruit, grape seed, cassia seed, beta-carrotene, VA, chrysanthemum flower and dendrobium.
US20060211723 Aporphine and oxoaporphine compounds and pharmaceutical use thereof The invention provides aporphine and oxoaporphine compounds that may be used to manufacture a medicaments for preventing or treating vascular dysfunctions that may result in ischemic and metabolic diseases or preventing complications associated with these diseases in human and mammal. The ischemic diseases may include ischemic cerebral apoplexy, ischemic cerebral thrombosis, ischemic cerebral embolism, hypoxic ischemic encephlopathy, ischemic cardiac disease or ischemic enteropathy etc. The metabolic disease may include diabetes-induced vascular diseases, such as hypertension, atherosclerosis, peripheral artery or venous thrombosis, retinopathy and nephropathy. Methods for treating ischemic and metabolic diseases or preventing complications are also disclosed.
US7419967 e.g. hexahydrofuro[2,3-b]furan-3-yl N-((1S,2R)-1-benzyl-3-(cyclopentyloxy)[(3-[2-(dimethylamino)ethyl]aminophenyl)sulfonyl]amino-2-hydroxypropyl)carbamate; against human immunodeficiency virus, chronic and acute viral infections The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
CN101991862B Cyclodextrin-polyethyleneimine-mediated supramolecular delivery system and preparation method The invention relates to a carrier of non-virogene transfection, in particular to a cyclodextrin-polyethyleneimine material-mediated supramolecular delivery system, and aiming to provide a novel supramolecular delivery system for non-virogene treatment and medicine synergistic treatment. The supramolecular delivery system is formed through combining polyethyleneimine-cyclodextrin with adamantane-adriamycin by utilizing a self-assembly principle with the polyethyleneimine-cyclodextrin as a framework and the adamantane-adriamycin as a core. The supramolecular delivery system has the advantages that a self-assembled composite can reduce toxic and side effects of adriamycin, simultaneously improve the bioavailability of adriamycin and can carry out synergistic effect together with a gene carried by the polyethyleneimine-cyclodextrin.
WO2008113095A1 Compositions and therapies comprising tranilast compounds and angiotensin-converting enzyme (ace) inhibitors and/or angiotensin receptor blockers (arb) The invention relates generally to compositions, methods and uses of at least one tranilast compound and at least one angiotensin-converting enzyme inhibitor and/or angiotensin receptor blocker.
US20090263388 Methods of preventing or treating cardiovascular, cerebrovascular and thrombotic disorders with tumor necrosis factor antagonists A method of treating or preventing a cardiovascular and/or a cerebrovascular disorder in an individual is disclosed. Also disclosed is a method for treating and/or preventing a thrombotic disorder in an individual. Further disclosed is a method of decreasing plasma fibrinogen in an individual.
US20110217300 Quinazolinone Compounds and Methods of Use Thereof The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a quinazolinone compound of the present invention
WO2014072647A1 Co-micronisation product comprising a selective progesterone-receptor modulator The invention relates to a co-micronisation product comprising: an active principle selected from the group containing selective progesterone-receptor modulators, metabolites thereof and mixtures of same and an N-vinyl-2-pyrrolidone-based polymer vehicle. The invention also relates to a pharmaceutical composition comprising the co-micronisation product and to the therapeutic uses thereof.
CN102698250A Injection for alcoholic liver and fatty liver The invention relates to the technical field of medicines, in particular to injection for alcoholic liver and fatty liver. The injection in each dosage comprises glutathione, tauric acid, 400 to 600mg of MgSO4, Minophagen-C, vitamin B complex, Vit B6, Vit B12 and Vit C in a certain ratio. The glutathione in the formula can protect liver cell membranes and scavenge free radicals; tauric acid is matched with the Minophagen-C and the MgSO4 to clear fat in liver and restore liver functions; and the injection can clear the fat in the liver and restore the liver functions in a short time, and has the advantages of short treatment course, quick response and no toxic or side effect compared with the conventional treatment scheme.
US6887676 For diagnosis/therapy/prevention of Creutzfeldt-Jacob disease The invention relates to methods and materials for use in the typing, diagnosis, prevention and/or treatment of prion disease.
CN103371981A Compound repaglinide-metformin hydrochloride solid quick-release preparation and preparation method and application thereof The invention relates to a compound repaglinide-metformin hydrochloride solid quick-release preparation and a preparation method and an application thereof, and belongs to the technical field of medicines. A quick-release tablet is prepared from repaglinide and metformin hydrochloride which are taken as medicinal active components, and suitable medicinal auxiliary materials, and the problems of quick dissolution-out of the indissolvable medicine, namely, repaglinide and the stability of the repaglinide in a tablet placement process are solved. The preparation method comprises the following steps of: respectively granulating the repaglinide and the metformin hydrochloride by selecting the suitable medicinal auxiliary materials; mixing, and then pressing into tablets, or filling into capsules. The prepared compound preparation has a synergetic effect on controlling blood sugar and improving the curative effect and is convenient for patients to take.
WO2008013987A3 N-alkyl substituted piperazinylmethylquinazolinones and azepanylmethylquinazolinones Compounds represented by Structural Formula (I) : are useful, for example, in the effective killing or reduction in rate of proliferation of cancer cells, such as in patients suffering from cancer. In addition to the compounds themselves, the invention provides pharmaceutical compositions of the compounds and method of treatment using the compounds.
CN103599108A Application of oleanolic acid in preparing medicament for preventing and treating cholestasis The invention discloses an application of oleanolic acid in preparing a medicament for preventing and treating cholestasis. A mouse with liver injury caused by over administration of lithocholic acid through experiments is used as a model, 5-20mg/kg oleanolic acid is administrated in a synergetic manner, the liver injury can be effectively alleviated and the level of bile acid can be reduced, the particular effect are that the survival rate of the mouse is remarkably increased, the activity of ALT (glutamic-pyruvic transaminase), AST (glutamic oxalacetic transaminase) and ALP (alkaline phosphatase) in serum is remarkably reduced, the necrosis degree of liver tissues is remarkably alleviated, and the content of total bile acid in liver is remarkably reduced. Liver gene and protein expression analysis prove that the oleanolic acid can remarkably up-regulate the expression of Mrp2, Mrp3 and Mrp4 and activate Nrf2, but does not have remarkable influence to other bile acid transporters and metabolic enzymes. Results indicate that the oleanolic acid can prevent and treat cholestasis liver injury induced by lithocholic acid, and the mechanism relates to a pathway of Nrf2-Mrps.
CN101897698A Sugar-lowering drug composition containing vildagliptin and B vitamins and application thereof The invention relates to a sugar-lowering drug composition and application thereof. The composition comprises 1) medicinal dosage of vildagliptin and 2) medicinal dosage of B vitamins. The invention relates to application of the sugar-lowering drug composition to preparing the drugs for treating and/or preventing diabetes or diabetic complications. The composition can effectively control the blood sugar, protect the endothelial cell functions in a synergic manner and reduce diabetic complications.
WO2006109680A1 Use of 3,5-diphenylpyrazole analogue as anti-tumor agent A growth inhibitory agent for tumor cells comprising a 3,5-diphenylpyrazole analogue represented by the general formula (1) or a pharmacologically acceptable salt thereof as the active ingredient: (1) wherein the group A represents a hydrogen atom, a carbonyl group or a sulfonyl group; the group J represents a lower alkyl group which may have a substituent or an amino group which may have a substituent; the groups G and Z independently represent a hydrogen atom, a hydroxyl group or the like; and the groups D, E, L, Q, X and Y independently represent a hydrogen atom, an aminocarbonyl group which may have a substituent, a lower alkoxycarbonyl group or the like.
US20100286231 Method for identifying a renal fibrosis process use of snail- activity-inhibiting compounds in the production of pharmaceutical compositions, method for identifying said inhibiting compounds, said pharmaceutical compositions and applications thereof The present invention relates to Snail, which is a protein that is directly involved in the etiopathogeny of renal fibrosis, in addition to being a marker of this disease. Therefore, the identification thereof may be used as a diagnosis for renal fibrosis. On the other hand, the Snail protein may be of great utility in identifying new drugs for the treatment of renal fibrosis, and its gene inhibition may be of use as a form of treatment in accordance with the present invention.
EP1714646A1 Pharmaceutical composition containing bakuchiol for treating osteoporosis in women The present invention discloses a novel use of bakuchiol or an extract containing bakuchiol in preventing or treating a woman suffering osteoporosis. An embodiment of this novel use is a pharmaceutical composition containing bakuchiol or an extract containig bakuchiol, which can be in the dosage forms of topical use, oral administration, injection or sustained release.
US20120010188 Imidazopyridine Compounds The invention relates to compounds of formula (I): and their pharmaceutically acceptable salts and solvates, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.
CA2665924A1 Piperidinylamino-pyridazines and their use as fast dissociating dopamine 2 receptor antagonists The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
CN102008449B Lansoprazole enteric pellet and preparation method thereof The invention discloses a Lansoprazole enteric pellet with improved stability and in-vitro release and a preparation method thereof. The Lansoprazole enteric pellet comprises the following components in parts by weight: 1-5 parts of acidifying or alkalizing agent, 80-200 parts of water, 2-8 parts of binder, 15-30 parts of Lansoprazole, a defined amount of defoamer, 0.5-5 parts of solubilizer, 50-200 parts of Celphere, and the balance of contagion gown and enteric coating. According to the invention, the technical problems of low dose, low release in buffer solutions, unstable medicine storageand the like are solved.
US7820178 VEGF isoforms and their use as anti-angiogenic, anti-vasodilatory, anti-permeability and anti-proliferative agents An isolated VEGF polypeptide having anti-angiogenic activity, said polypeptide including the amino acid sequence of SEQ. ID NO. 1, or variants thereof.
CN102178669A Application of oleic acid to preparation of anti-HPV (Human Papilloma Virus) drugs The invention provides application of oleic acid to preparation of anti-HPV (Human Papilloma Virus) drugs.
EP1322316B1 Diuretic or sulphonylurea for use in antiviral treatment A diuretic, e.g. loop diuretic or thiazide, or a sulphylurea is useful in the treatment of DNA viral infections.
US20100029567 Method of correcting imbalance between bone resorption and bone formation and kits and compositions therefor Compounds, methods, uses, compositions, kits and packages for the treatment of imbalance between bone resorption and bone formation, based on uses of 4-phenyl-2 propionamidotetralin (4-P-PDOT) and analogs, derivatives, prodrugs, precursors thereof, and salts thereof, are described.
CN101332201A Anticancer composition containing irinotecan An anti-cancer combination containing irinotecan is a sustained-release injection, which contains a sustained-release microsphere and a menstruum. The sustained-release microsphere contains PI3Ki and/or topoisomerase inhibitor and sustained-release auxiliary materials; the menstruum is an ordinary menstruum or a special menstruum containing a suspending agent. The viscocity of the suspending agent is 100cp to 3000cp (at the temperature of 20 DEG to 30 DEG) and the suspending agent is selected from carboxymethylcellulose sodium, etc. The sustained-release auxiliary materials are selected from a polyphosphonate copolymer of p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP/TC), p(BHET-EOP/TC ), p(BHDPT-EOP/TC), p(BHDPT-EOP/TC), p(CHDM-HOP) or p(CHDM-EOP), and the like, or a copolymer of polyphosphate ester and polylactic acid, polifeprosan, dienoic fatty acid or decanedioic acid, or a copolymer or a mixture of p(erucic acid dimer-decanedioic acid) or a copolymer or a mixture of p(boletic acid-decanedioic acid). The anti-cancer combination can also be made into a sustained-release implanting agent, which can be injected or placed in or around tumor to maintain the effective medicine density for more than 40 days. The anti-cancer combination can also obviously reduce the general reaction of the medicine and selectively enhance the curing effect of non-operational therapies such as radiotherapy and chemotherapy.
WO2010118200A3 Liposomal formulations of tocopheryl amides Formulations of N-chroman dicarboxylic acid derivatives and their bioisosteres in liposomal systems. Lyophilized liposomal dosage forms of N-chromans, are found to be stable, to achieve therapeutically meaningful plasma levels on administration to a mammalian host, and to demonstrate selective pro-apoptotic oncolytic properties in vivo. Advantageously, these formulations overcome the systemic toxicity that characterized their administration by other dosage forms.
CA2673164A1 Derivatives of azabicyclo octane, the method of making them and the uses thereof as inhibitors of dipeptidyl peptidase iv Derivatives of azabicyclo octane presented by formula (I), the method of making them, and the compositions containing the same and the uses thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV), wherein the substitutes in formula (I) have the same meanings as what is mentioned in the descriptions.
CN101095743A Exterior-applied medicine composition for treating gynecologic diseases and method of making the same and the use thereof The invention relates to an externally-used Chinese preparation for treating gynaecologic diseases and process for preparation, which comprises the following components (by weight ratio): yellow corktree bark 5-40 parts, borneol 0.1-10 parts, mercury monochloride 1-10 parts, orpiment 0.1-10 parts and centipede 0.1-6 parts. The medicament can be prepared into externally-used common medicinal herble usual dose through the conventional preparing processes.
WO2012123938A1 Quinolone analogs for treating autoimmune diseases Provided are methods of treating autoimmune diseases by administering to the subject a therapeutically effective amount of a quinolone compound such as 2-(4- methyl- 1,4-diazepan- 1 -yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H- benzo[4,5]thiazolo[3,2-a][l,8]naphthyridine-6-carboxamide (CX-5461). Also provided are methods of monitoring efficiency of treatment of the quinolone compound by determining the expression level of at least one gene of the RNA polymerase I pathway.
US20080286220 Hair Treatment Compositions Comprising A Disaccharide, A Di-Acid And A Source Of Ammonium Ions The invention provides a hair treatment composition comprising i) a disaccharide; ii) a di-acid, and iii) a source of ammonium ions.
US20090118215 Bioresorbable Controlled-Release Composition A novel method for the preparation of a highly densified and at least partly, preferably fully or almost fully hydrated ceramic for use in the preparation of a pharmaceutical composition notably for controlled-release of one or more therapeutically, prophylactically and/or diagnostically active substance. The method involves a concomitant step of hydrating and densifying a bioresorbable and hydratable ceramic such as calcium sulphate. The invention also relates to compositions comprising such a highly densified ceramic. The pharmaceutical composition is useful for targeted and controlled local prolonged release of active substances, e.g. anti-cancer agents, whereby the spectrum and severity of side effects are minimized due to an optimized local concentration-time profile.
CN101972240B Modafinil composition The invention relates to a modafini composition. Co-crystals and solvates of racemic, enantiomerically pure, and enantiomerically mixed modafinil are formed and several important physical properties are modulated in the invention. The solubility, dissolution, bioavailability, dose response and stability of modafinil can be modulated so as to improve the efficacy in pharmaceutical compositions.
CN102764233A Liposome injection of 3-amino-6-aryl-thieno[2,3-b]pyridine-2-methanamide derivatives and preparation technology thereof The invention discloses a liposome injection of two derivative compounds, namely 3-amino-6-aryl-thieno[2,3-b]pyridine-2-methanamide derivative compound 1 and compound 2 and a preparation technology thereof. The compounds have specific in vitro and in vivo liver cancer inhibition effects, but are insoluble in water and have poor oral absorption and low plasma concentration. Therefore, the compounds are made into the liposome injection which comprises the following components of: by weight, 0.01-0.6% of the compound 1 (or 2), 0.01-5% of soya lecithin or hydrogenated soya lecithin, 0.001-1.5% of cholesterol and 0-1.5% of macrogol ester. The preparation technology comprises the following steps of: 1) lipid phase freeze-drying; 2) lipid film forming; 3) lipid phase hydration; 4) liposome multigelation; and 5) liposome homogenization. The solubility of the compounds in the obtained liposome is increased by 3 orders of magnitude in comparison with that of the compounds in water. In addition, the particle size is small and diameter distribution is narrow. After intravenous infusion of the liposome injection, the initial plasma concentration is raised by about 30 times in comparison with that of a corresponding oral preparation. And the liposome injection of the two derivative compounds is an ideal preparation of the series of compounds.
US20120202832 Kinase inhibitors, prodrug forms thereof and their use in therapy The invention provides kinase inhibitors of Formula I: wherein either: (1) R1 is H, and (a) R2 is (3-chlorobenzyl)oxy- and R3 is chloro; (b) R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; (c) R2 is 2-pyridinylmethoxy and R3 is chloro; (d) R2 and R3 are both chloro; (e) R2 is chloro and R1 is bromo; (f) R2 and R3 are both bromo; (g) R2 is fluoro and R3 is ethynyl; (h) R2 is chloro and R3 is ethynyl; (i) R2 is bromo and R3 is ethynyl; (j) other than when R1 is in the 3-position in combination with R3, in the 4-position, R2 is bromo and R3 is fluoro; (k) R2 is 2-pyridinylmethoxy and R3 is fluoro; or (l) R2 is 2-pyridinylmethoxy and R1 is bromo; or (2) at least one of R1, R2 and R3 is selected from benzyloxy, 3-chlorobenzyloxy and 2-pyridinylmethoxy and when at least one of R1, R2 and R3 is not benzyloxy, 3-chlorobenzyloxy or 2-pyridinylmethoxy, each of the others is independently selected from H, halogen, and C2-C4 alkynyl, with the proviso that when one of R1, R2 and R3 is benzyloxy or 2-pyridinylmethoxy, the other two of R1, R2 and R3 are not H; or (3) two of R1, R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; and the other is selected from H, halogen and C2-C4 alkynyl. Also provided are reductive prodrugs, comprising a kinase inhibitor as defined above and a reductive trigger linked directly or indirectly to a nitrogen of the kinase inhibitor. Further provided are pharmaceutical compositions, comprising the kinase inhibitors or the prodrugs, and the use of such compositions in therapy, in particular for treating cancer.
CN103087026A Crystal form D of 7-hydroxyl isoflavone, preparation method of crystal form D and medicine composition and use of crystal form D The invention discloses five crystal forms of 7- hydroxyl isoflavone, preparation methods of crystal forms and medicine compositions and uses of crystal forms. Specifically, the invention relates to the crystal form A, the crystal form B, the crystal form C, the crystal form D and the crystal form E, which exist under a solid state, of the 7-hydroxyl isoflavone, relates to the preparation methods for preparing the samples of the five crystal forms, relates to various preparations which are prepared and developed by using different crystal form substances of the 7-hydroxyl isoflavone as active ingredients, as well as the dominant clinical treatment action of the medicine compositions of the preparations in preventing cardiovascular and cerebrovascular diseases, osteoporosis, inflammation, metabolic diseases and other diseases. The crystal forms can be used for affecting the absorption rate of the solid medicine active ingredients in the living body, and reinforcing or reducing the plasma drug concentration in the living body, thereby affecting the clinical treatment action of the medicines.
CN101092417B Folacin analogue, and salt of folacin analogue in use for medical treatment This invention discloses folic acid analogues as shown in general chemical formula (I), and their salts used in therapy. In general chemical formula (I), R is OH, Cl, NH2, OCH3 or OCH2CH3. This invention also discloses the application of the folic acid analogues and their salts in drugs for treating cancers. The folic acid analogues and their salts have strong inhibitive activity on the growth of multiple cancer cells.
EP2125753A1 Fused heterocyclic compounds having crf antagonistic activity There is provided a compound of the formula: wherein R1 is an optionally substituted hydrocarbyl, a substituted amino, etc.; R2 is an aromatic group substituted with one or two substituents at the positions adjacent to the position bonded to Z, and said aromatic group may have additional substituent(s); X is -NR3- wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl, or sulfur; Y1, Y2 and Y3 are an optionally substituted methine or a nitrogen, etc.; and Z is an optionally substituted methylene, provided that carbonyl is excluded; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.
CN102935087A Compound electrolyte injection composition and preparation method thereof The invention relates to a preparation method of compound electrolyte injection and a compound electrolyte injection composition. The preparation method comprises the following steps of: adding water for injection of which the quantity is 50% as heavy as the quantity of the prescription quantity in a concentrated preparation tank, weighing sodium chloride, sodium gluconate, sodium acetate, potassium chloride and magnesium chloride of which the quantity is equal to the quantity of the prescription quantity and putting into a liquid preparation tank, dissolving in a stirring way, adding 0.1% (g/ml) of active carbon for injection, adsorbing for 15min in a stewing way, removing carbon into a dilute preparation tank in a filtering way, additively adding water for injection to be near to be full dose, evenly stirring, adjusting pH to be within the range from 7.0 to 7.6 by 0.1mol/L of sodium hydroxide, finely filtering by filters with 0.45mum and 0.22mum after an intermediate is detected to be qualified, carrying out light detection till no foreign matters are visible, carrying out split charging according to 500ml of each bag, sterilizing for 15min in a hot-press way under 121 DEG C, printing after the products are detected to be qualified under light, packing, and storing. Every 1000mL of the compound electrolyte injection composition prepared by the preparation method comprises 5.26g of sodium chloride, 5.02g of sodium gluconate, 3.68g of sodium acetate, 0.37g of potassium chloride and 0.30g of magnesium chloride; and the pH value is 6.8-7.4. The toxins, the insoluble particles and the heavy metals in the composition bacterium completely meet the requirements of injection.
WO2013082562A1 Prebiotic formulations and methods of use Provided are methods and pharmaceutical compositions for treating symptoms associated with lactose intolerance and for overall improvement in gastrointestinal health. Described herein are methods and pharmaceutical compositions for improving overall gastrointestinal health or for decreasing symptoms of lactose intolerance by administering to subject in need thereof a pharmaceutical composition comprising a prebiotic, optionally in combination with effective amount of a probiotic microbe or microbes.
US20110110965 Compositions that induce t cell help The present invention relates, at least in part, to compositions, and related methods, comprising MHC II binding peptides. In one embodiment, the MHC II binding peptides comprise a peptide having at least 70% identity to a natural HLA-DP binding peptide, HLA-DQ binding peptide, or HLA-DR binding peptide.
WO2010098286A1 Pharmaceutical preparation containing mineralcorticoid receptor antagonist Disclosed is a therapeutic agent for diabetic nephropathy, which can exhibit an excellent inhibitory activity on the increase in the quantity of proteins in urine. Specifically disclosed is a pharmaceutical preparation containing a mineralcorticoid receptor antagonist as an active ingredient.
US20100278937 Compositions and methods to prevent and/or treat cancer with pa-card The present invention relates to methods and materials for killing cancer cells with proteins derived from bacteria. The invention specifically relates to Azurin, Laz, Pa-CARD, and fusion proteins Azu-H.8 and H.8-Azu, and their use in killing leukemia cells and/or ovarian cancer cells.
CN101225383B RNA interference sequence and recombinant interference plasmid of fucosyl transferase I and IV for suppressing synthesis of LeY carbohydrate antigen The present invention relates to a RNA interference sequence and a restructuring interference plasmid of the fucosyltransferase I and IV used for inhibiting the synthesis of LeY saccharide antigen, which mainly comprises: the DNA sequence of seven FUT1/FUT4 SiRNA templates of fucosyltransferase I and seven FUT1/FUT4 SiRNA templates of fucosyltransferase IV are screened, seven FUT1 and seven FUT4 restructuring interference plasmid are respectively constructed on the base of polyclonal specific enzyme cutting sites of the RNA interference carried (pSilencer-4.1-CMV neo), and the interference plasmid is used as antitumor drugs. The RNA interference sequence and a restructuring interference plasmid of the fucosyltransferase I and IV used for inhibiting the synthesis of LeY saccharide antigen has the advantages of obvious function of inhibiting tumor growing, high efficiency, high safety and economic tumor gene therapeutic mode.
CN102827160A PI3K or PI3K/m-TOR pathway inhibitor and pharmaceutical applications thereof The invention discloses a compound which is a PI3K or PI3K/m-TOR pathway inhibitor. The invention also provides pharmaceutical ingredient and preparations containing the compound, and the applications of the PI3K or PI3K/m-TOR pathway inhibitor. The compound can be independently administrated, or can be used together with other compounds, for treating tumors.
CN101757021A Compound infusion preparation applicable to canine fluid infusion and preparation method thereof The invention discloses a compound infusion preparation applicable to canine fluid infusion and a preparation method thereof and relates to a compound infusion product, in particular to a compound product applicable to the canine fluid infusion. The compound infusion preparation in each 100 parts of injection water comprises 0.1 to 0.5 part of commercially-available pharmaceutical-grade sodium chloride, 0.05 to 0.3 part of potassium chloride, 0.05 to 0.4 part of sodium bicarbonate and 0.5 to 5 parts of glucose. The preparation method comprises the following steps: firstly, dissolving the sodium chloride, the potassium chloride, the sodium bicarbonate and the glucose in a proper amount of injection water at the normal temperature; secondly, adding the injection water into the mixture to make 100 parts of solution; thirdly, performing routine filtering by using a 0.22 ul microporous membrane; fourthly, filling according to an infusion bottle with 100 ml specification by using a liquid filling machine; and finally, sterilizing the filtrate at the high temperature of 121 DEG C for 20 minutes to obtain a finished product. When used, the compound infusion preparation can be directly used for the canine infusion and the liquid infusion for hypohydration symptom caused by various diseases of the canine.
EP1292278B1 Preparations that contain an extract of the plant pistia stratiotes The invention relates to preparations that contain an extract of the plant Pistia stratiotes.
WO2013187575A1 Composition comprising hypothemycin as active ingredient for preventing and treating macrophage activation syndrome, hepatocirrhosis, or obesity The present invention relates to a pharmaceutical composition or health food comprising hypothemycin as an active ingredient for preventing and treating macrophage activation syndrome, hepatocirrhosis, or obesity. More particularly, since hypothemycin according to the present invention inhibits the production of TNF-α and the expression of TNF-α mRNA caused by activated macrophages, hypothemycin can be effectively used as an active ingredient for a pharmaceutical composition or health food for preventing and treating macrophage activation syndrome, hepatocirrhosis, or obesity, which are diseases induced by activated macrophages.
US20110190320 Compositions for Treating or Delaying the Onset of Hair Loss Disclosed herein are novel methods and compositions for treating and/or preventing hair loss in patients. Specifically exemplified herein are compositions containing a modified pyrimidine that are topically applied to a scalp of an patient. Typically, the patient has androgenic alopecia, alopecia greata, postpartum alopecia or telogen effluvium.
US20110236435 ENHANCED BONE CELLS GROWTH AND PROLIFERATION ON TiO2 NANOTUBULAR SUBSTRATES TREATED BY RADIO-FREQUENCY PLASMA DISCHARGE A method for growing bone cells. In one aspect, the present invention provides a method for growing bone cells, comprising the steps of (a) anodizing a titanium substrate to form an array of titanium dioxide nanotubes on a surface of the titanium substrate, (b) subjecting the anodized titanium substrate to a radio frequency plasma discharge to chemically modify the array of titanium dioxide nanotubes formed on the surface of the titanium substrate, (c) seeding bone cells onto the surface of the titanium substrate that has an array of titanium dioxide nanotubes thereon after the subjecting step, and (d) incubating the seeded bone cells for a period of time effective for the cells to grow and proliferate.
US20090098081 System for providing a method for applying a skin sealant having a phase change visual indicating component A system for providing a method of sealing skin with a film forming polymer is provided. The system includes providing an at least two part applicator containing a sealant composition in one or more frangible containers, providing instructions for using the applicator associated therewith, where the method including moving at least one of said applicator parts from a first position to a second position and applying said sealant to skin. The composition has film former, a plasticizer and 3000 to 10000 ppm of a dye that changes color when is undergoes a phase change. The color change is visible to a human eye under normal light conditions. changing dyes may be used to indicate that the composition has dried. The dyes change color in response to the phase change, i.e., drying of the film former. The dye may be added either directly to the composition, incorporated into a sponge on an applicator through which the composition is dispensed and applied, applied separately or applied simultaneously from a separate reservoir. The amount of dye in the composition can be adjusted to provide a visual cue to the user of the application area and the extent of cure though should generally be in the range of 3000 to 10000 ppm.
US20110243894 Methods of treating hepatitis c virus infection The present invention provides methods of treating hepatitis C virus (HCV) infection; methods of reducing the incidence of complications associated with HCV and cirrhosis of the liver; and methods of reducing viral load, or reducing the time to viral clearance, or reducing morbidity or mortality in the clinical outcomes, in patients suffering from HCV infection. Also provided are methods of treating liver steatosis and liver fibrosis.
CN101020688A 1-(3-indolyl)-1,2,3,4-tetrahydro-beta-carboline derivative and its prepn and use The present invention belongs to the field of medicine synthesis technology, and is especially 1- (3-indolyl)-1, 2, 3, 4-tetrahydro-beta-carboline compounds and analogs in the general expression as shown and with substituted hydroxyl radical or acyl radical in the 2nd position, and their preparation process and medical application. Initial pharmacodynamic research of extracorporeal rice blast mold resisting experiment and extracorporeal antitumor experiment shows that these compounds has excellent antifungal activity and antitumor activity, so that they may be developed into antifungal medicine and antitumor medicine.
CN1943625A Oral sterilizing liquid The invention belongs to technical field of oral sterilization , is a sterilized therapeutic solution for oral hygiene , comprising the following components according to percent by weight: sweeting agent 0.1-1%,the root of large-flowered skillcap 0.1-1%, dried alum 0.1-1%, honeysuckle 0.1-1%, vitamin E 0.1-1%, metronidazole 0.1-0.5%, amoxicillin 0.1- 0.5%,glycerine 1-3%, 85% of density alcohol 5-10%,the remaining being distilled water; grinding the root of large-flowered skillcap, dried alum and honeysuckle separately and sifting out with 20 mesh, adding alcohol separately into powdered article and immersing at temp. 4deg.C for 48- 72 hr, thereafter filtering in the , freezing filter liquor to dry at temp. 4deg.C separately and obtaining extracts; again mixing said extracts with left components, adding medicinal phosphoric acid adjusting pH till reaching 7.0-7.5, finally canned and sealed.
CN101502497A Fenofibrate medicament composition The invention relates to a fibrate drug combination and solves the problem of the low bioavailability of fenofibrate. The drug combination comprises the following materials according to part by weight: 6 to 42 parts of fenofibrate, 60 to 80 parts of polyethylene glycol 6000 or poloxamer 407, 6 to 42 parts of compritol 888 ATO or precirol AT05, 2 to 12 parts of polyethylene glycol glyceryl dilaurate or ethylene glycol monoethyl ether and 2 to 12 parts of cremophor RH40 or cremophor EL. The invention can finish the processes of drug micronization and micronized drug dispersion in one-step operation based on the physical and chemical properties of raw materials and auxiliary materials; the compritol 888 ATO can achieve the purpose of sustaining the drug release owing to the hydrophobicity thereof, and the compritol 888 ATO has the release characteristics of zero-order sustained release at a particular ratio in a continuous and complete state; the hydrophilic matrix formed by polyethylene glycol 6000 can prevent the drug release from being affected by acid and alkali and reduce the possibility of bioavailability difference caused by the individual difference; and the invention has the advantages of simple production process, low cost and controllable quality.
CN103483352A Medicinal bulk drug for resisting tumors The invention relates to a medicinal bulk drug for resisting tumors, and in particular relates to a bulk drug for medicines. The active component of the bulk drug is a compound in the formula I or pharmaceutical salt thereof, wherein each substituent is described as the specification. The invention also relates to a medicinal composition containing the compound in the formula I or salt thereof, a preparation method of the medicinal composition and pharmaceutical application thereof. The bulk drug has excellent characteristics, such as stability and safety, when serving as an anti-tumor drug.
US7816317 Tripeptide prodrug compounds The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide of three amino acids, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by a trouase enzyme such as Thimet oligopeptidase. Also disclosed are methods of making and using the prodrug compounds.
CN101269039A Levorotation carnitine sustained-release dropping pill and preparation method thereof The invention relates to a drug for treating adiposis and hepatopatic diseases and particularly relates to a drug compound oral pharmaceutical formulation adopting L-carnitine (or L-carnitine salts) as drug active ingredient and having the effects of reducing weight and inhibiting hepatopatic diseases. The drug aims to supplement the deficiency of the prior art and provide a sustained-release L-carnitine dropping pill formulation. The sustained-release L-carnitine dropping pill is prepared by adding stabilize Vitamin E to the ingredients accepted in the prior art to guarantee no occurrence of an obvious change related to the substance content for the drug during the effective storage period and has the advantages of full release, controllable release time and high bioavailability simultaneously. The sustained-release L-carnitine dropping pill is suitable for clinical and family use.
WO2009120191A1 Process for the preparation of benzo-fused heteroaryl sulfamates and crystalline form of n- ( ( (2s) -6-chloro-2,3-dihydro-l,4-benzodioxin-2-yl) methyl-sulfamide The present invention is directed to a process for the preparation of benzo-fused heteroaryl sulfamates, useful for the treatment of epilepsy and related disorders according to formula (IA) and to a crystalline compound of formula (I-S). Process for the preparation of a compound of formula (IA).
CN101406447A Technique for preparing compound ceftiofur oil suspension injection The invention discloses a preparation process for compound recipe ceftiofur oil suspensoid injection. The preparation process comprises the following steps: (1) taking neutral soybean oil, filtrating, heating and sterilizing and cooling down the soybean oil, adding aluminum stearate into the soybean oil to prepare gel, diluting the gel into factice of 2+-0.2 percent through the filtrated and sterilized soybean oil, and filtrating the factice through a No.3 sintered glass funnel for standby; and (2) taking hydrochloric acid ceftiofur/sulbactam according to a recipe, mixing the hydrochloric acid ceftiofur/sulbactam with the factice, grinding the mixture, adding lecithin into the mixture till the mixture is ground evenly, and then obtaining the compound recipe ceftiofur oil suspensoid injection through shifting the ground hydrochloric acid ceftiofur/sulbactam into a graduated cylinder and so on. As the invention adopts the preparation method, compared with a single recipe ceftiofur preparation, the compound recipe ceftiofur oil suspensoid injection has the advantage that the compound recipe ceftiofur oil suspensoid injection has antibacterial activity against bacteria capable of resisting the single recipe ceftiofur, that is, the compound recipe ceftiofur oil suspensoid injection can effectively treat bacterial infection generating ESBLs.
US20080260821 Berry Preparations and Extracts A method for deriving compositions having antioxidant and anti-inflammatory activity from berries is provided. The method results in a berry extract compositions having stable anthocyanin content. In one aspect, the method comprises exposing a berry to a solvent composition having a pH of from about 1 to about 4.5, and recovering a berry extract having a stabilized anthocyanin content. The berry may be a blackberry. A cryoprotectant may be added, to further stabilize the anthocyanin content. Compositions comprising the berry extract of the present invention, formulated for oral and/or topical administration, are provided also, including nutritional supplements, capsules, enteric-coated capsules, film-coated capsules, tablets, enteric-coated tablets, film-coated tablets, chewing gums, lotions, creams, mucoadhesive gels, vanishing lotions, vanishing creams, and the like. In yet another aspect, the present invention provides methods and compositions for treating inflammation, oxidative damage, or cancer in a mammal.
US20100028413 Skin treatment strip The skin treatment strip includes a base liner and an applicant liner coupled to the base liner by an adhesive. The skin treatment strip further includes a chemical layer sandwiched between the base liner and the applicant liner that is reactive to a skin blemish. The chemical layer includes a weak acid such as hydrogen peroxide for treating the skin blemish, a base such as sodium hydroxide for balancing skin pH and preventing skin irritation, a sugar-based alcohol such as glycerin for soothing the skin and a water-based carrier. Preferably, the adhesive is used to maintain contact of the chemical layer with the skin blemish upon application of the applicant liner.
US20100298370 Benzothiazolyl thienopyridine derivatives and uses thereof Novel benzothiazolyl thienopyridine compounds are provided and pharmaceutical compositions comprising benzothiazolyl thienopyridine compounds. The benzothiazolyl thienopyridine compounds are capable of inhibiting the interactions between vascular endothelial growth factor (VEGF) and heparan sulfate glycosaminoglycans (HS-GAGs), and are useful for prevention or treatment of diseases and disorders such as inflammation, autoimmune diseases and cancer.
US20090028941 Pulsatile gastric retentive dosage forms Dosage forms for delayed and pulsed release of therapeutic agents into the stomach are described. The dosage forms are gastric retentive dosage forms that achieve release of the therapeutic agent into the stomach and upper gastrointestinal tract subsequent to administration of the dosage form. The dosage forms find particular use in administration of acid-labile active agents such as proton pump inhibitors, and in treating gastric acid secretion such as gastro-esophageal reflux disease (GERD) and nocturnal acid breakthrough (NAB).
US20110262425 Therapeutic agent for mll leukemia and moz leukemia of which molecular target is m-csf receptor, and use thereof An objective of the present invention is to provide therapeutic agents for MLL leukemia and MOZ leukemia, which include an M-CSF receptor inhibitor as an active ingredient. Another objective of the present invention is to provide methods of screening for pharmaceutical compositions that treat or prevent leukemia by suppressing the expression or activity of M-CSF receptor. Still another objective of the present invention is to provide methods of testing for leukemia, which include the step of determining the expression level of an M-CSF receptor. The present inventors conducted dedicated studies, and as a result revealed that the M-CSF receptor (M-CSFR, CSF1R, c-FMS, or CD115) is highly expressed in cells having the activity of inducing MLL or MOZ leukemia (leukemia stem cells), both of which are intractable acute leukemia. Specifically, the present inventors discovered that the M-CSF receptor signal is closely associated with the leukemia onset.
US20100196319 4, 5-ring annulated indole derivatives for treating or preventing of hcv and related viral infections The present invention relates to 4,5-ring annulated indole derivatives of formula (I), compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient, wherein ring Z of formula (I), is cyclohexyl, cyclohexenyl, 6-membered heterocycloalkyl, 6-membered heterocycloalkenyl, 6-membered aryl or 6-membered heteroaryl, wherein R1, R2, R3, R6, R7 and R10 are as described herein.
US20120315219 Drug Delivery Coating For Use With A Stent A coated medical device and a method of providing a coating on an implantable medical device result in a medical device having a bio-absorbable coating. The coating includes a bio-absorbable carrier component. In addition to the bio-absorbable carrier component, a therapeutic agent component can also be provided. The coated medical device is implantable in a patient to effect controlled delivery of the coating, including the therapeutic agent, to the patient.
CN102675211A Synthetization of secnidazole cinnamate derivative, and applications of secnidazole cinnamate derivative on antibacterial agent The invention provides a secnidazole cinnamate derivative which has the following general formula, wherein R in the formula is shown in the description. The secnidazole cinnamate derivative can obviously inhibit the growth of gram positive bacteria and gram negative bacteria, thus being applicable in preparation of antibacterial drugs. The invention discloses a preparation method for the secnidazole cinnamate derivative.
CN203001479U Cetirizine hydrochloride tablet The utility model is suitable for the technical field of pharmacy, and provides a cetirizine hydrochloride tablet which is a special-shaped tablet with a notch disposed at the central part of the cetirizine hydrochloride tablet. According to the utility model, the cetirizine hydrochloride tablet is prepared into a special-shaped tablet with a notch disposed at the central part, and thus the drug dosage can be distributed with the notch as a boundary, which is accurate in dosage distribution and convenient for patients.
US7026335 Melanocortin receptor ligands The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring. The compounds, including all enatiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein preferably R is substituted aryl, W is a pendant unit having the formula: -L-Q L is a linking unit, Q is preferably a cyclic hydrocarbyl unit; W1 is preferably a carbocyclic unit and W2 is a heteroatom comprising unit.
EP1027349B1 Tetrahydrofuran phosphate- and hydroxy esters, as prodrugs for the corresponding antifungal agent A compound of formula (I) wherein G is H or PO3H2 or a pharmaceutical acceptable salt thereof, pharmaceutical compositions containing such compounds and method of using such compounds or pharmaceutical compositions containing them to treat or prevent fungal infection are disclosed.
WO2009150138A1 Novel oxadiazolyl-diazabicyclononane derivatives and their medical use This invention relates to novel oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment ofdiseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
US20100113429 Inhibitors of ftsz and uses thereof The invention relates to inhibitors of FtsZ polymerization and uses thereof.
US7425573 Use of annellated pyrrole compounds in the treatment of articular cartilage or subchondral bone degeneration Treating or preventing degeneration or destruction of articular cartilage and/or subchondral bone in the affected joint of a mammal is accomplished by administering a compound of formula (I), wherein the variables have the meanings given in the present description. A preferred compound of formula (I) is formula (II). This treatment ameliorates, diminishes, actively treats, reverses or prevents any injury, damage or loss of articular cartilage or subchondral bone subsequent to said early stage of said degeneration
WO2005026164A1 Pharmacologically active imidazo[4,5-c]pyridines The invention relates to 6-substituted imidazo[4,5-c]pyridines of formula 1, in which X is O (oxygen) or NH and Y has either the meaning -CH2-AR or Y denotes the group gp (gp) wherein Z has the meaning -CHR8- or -CHR8-CHR9-. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.
EP1604651A1 Transdermal patches and methods for delivering testosterone A method of providing testosterone replacement therapy to a woman in need of such therapy comprising applying a testosterone-delivering patch to the skin of said woman which patch transdermally delivers 50 to 500 µg/day of testosterone to the woman.
WO2008109368A3 Nucleic acid compounds for inhibiting vegfr gene expression and uses thereof The present disclosure provides meroduplex ribonucleic acid molecules (mdRNA) capable of decreasing or silencing VEGFR (e.g., FLTl, KDR, FLT4) gene expression. An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to a FLTl, KDR, or FLT4 mRNA. In addition, the meroduplex may have at least one uridine that is a 5-methyluridine, a locked nucleic acid, or optionally other modifications, and any combination thereof. Also provided are methods of decreasing expression of a VEGFR gene in a cell or in a subject to treat a VEGFR-related disease.
US20110053927 Nanoparticle formation via rapid precipitation The invention encompasses a method for making nano-sized particles of water-insoluble pharmaceuticals comprising: (1) dissolving the water-insoluble pharmaceutical in a water-miscible solvent, optionally with water and inactive pharmaceutical ingredients, to make a solution; (2) rapidly mixing the solution with an anti-solvent which creates a high level of supersaturation, wherein the anti-solvent is water with optional inactive pharmaceutical ingredients; (3) simultaneously applying energy to the resulting mixture during the mixing of solution and anti-solvent as nano-sized drug particles precipitate out and form a slurry mixture under supersaturation; and (4) optionally isolating the nano-sized particles of water-insoluble pharmaceuticals from the slurry mixture.
US20080300292 Nitrosated and Nitrosylated Compounds, Compositions and Methods for the Treatment of Ophthalmic Disorders The invention describes novel nitrosated and/or nitrosylated compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent. The invention also provides methods for treating ophthalmic disorders. The nitrosated and/or nitrosylated compounds are preferably nitrosated and/or nitrosylated (3-adrenergic antagonists and nitrosated and/or nitrosylated angiotensin-converting enzyme (ACE) inhibitors.
CA2390295C A method for chemoprevention of prostate cancer This invention relates to the chemoprevention of prostate cancer and, more particularly, to a method of suppressing or inhibiting latent prostate cancer comprising administering to a mammalian subject a chemopreventive agent and analogs and metabolites thereof. The chemopreventive agent prevents, prevents recurrence of, suppresses or inhibits prostate carcinogenesis; and treats prostate cancer.
US20080085282 Methods of detecting and controlling mucoid pseudomonas biofilm production Compositions and methods for detecting and controlling the conversion to mucoidy in Pseudomonas aeruginosa are disclosed. The present invention provides for detecting the switch from nonmucoid to mucoid state of P. aeruginosa by measuring mucE expression or MucE protein levels. The interaction between MucE and AlgW controls the switch to mucoidy in wild type P. aeruginosa. Also disclosed is an alginate biosynthesis heterologous expression system for use in screening candidate substances that inhibit conversion to mucoidy.
CN102892898A Diagnostic kit including micro-rna biomarkers and used for diagnosis of hepatocellular carcinoma, and method The invention provides micro-RNA biomarkers and a diagnostic kit including DNA molecules of the micro-RNA biomarkers of a plurality of codes. The diagnostic kit is used for identifying one or more target plasmas expressing hepatocellular carcinoma. The invention also provides a method for diagnosis and treatment of the hepatocellular carcinoma, and a medicinal composite for prevention and treatment of the hepatocellular carcinoma.
EP1309563B1 Heterocyclic-hydroxyimino-fluorenes and their use for inhibiting protein kinases Compunds of the formula I or II wherein X is CY or N, and W is O or S, modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
EP1740573A1 Amides as bace inhibitors The present invention provides BACE inhibitors of Formula (I): methods for their use, and intermediates and methods for their preparation.
CN102670932A Medicine for quickly removing wart The invention discloses a medicine for quickly removing wart. According to weight percent, the medicine comprises 15 to 25 percent of edible alkali, 55 to 65 percent of quicklime, 2 to 4 percent of green Chinese onion leaf and the balance of white spirit. The preparation process of the medicine for quickly removing the wart comprises the following steps of: selecting the edible alkali and the quicklime firstly according to the mixture ratio, also grinding into a powder shape, then mixing, stirring, afterwards adding the white spirit, stirring, adding the foamy green Chinese onion leaf finally, mixing fully and stirring into a paste shape. The medicine for quickly removing the wart has a simple process, is convenient to prepare and use and can be used for quickly curing various kinds of aural verruca, verruca plana, verruca plantaris, molluscum contagiosum and verruca filiformis.
CN1970061A Ointment for treating gastric disease and preparation process thereof The invention relates to a plaster for treating gastropathy and its preparing process, wherein the raw materials include rhizome of Sichuan lovage 4-6 parts, safflower 4-6 parts, rheum officinale 4-6 parts, rhizoma corydalis 9-11 parts, banksia rose 4-6 parts, cimicifuga rhizome 4-6 parts, cyprus longus 4-6 parts, amomum fruit 6.5-8.5 parts, clove 4-6 parts, cinnamon 4-6 parts, flavescent sophora root 4-6 parts, radish seeds 9-11 parts, frank incense 4-6 parts, myrrh 4-6 parts, camphor 1.5-3.5 parts, dried orange peel 4-6 parts, giant typhonium tuber 4-6 parts, pinellia tuber 4-6 parts, finger citron 9-11 parts, rhodojaponin 4-6 parts, cuttle-bone 4-6 parts, white peony root 9-11 parts.
US20080031929 Liquid bandage The present invention relates to hemostatic fabric materials, and to the methods for making and using such materials. In particular, the present invention relates to hemostatic fabric materials made from chemically treated plant materials that are soluble on wound surfaces.
CN101724043A Human epididymis expression sperm binding protein HEL-89, encoding gene and application thereof The invention belongs to the field of biotechnology and medicine, and discloses a new human epididymis specific expression sperm binding protein HEL-89 as well as preparation and application thereof. The invention discloses an amino acid sequence of the HEL-89 protein and provides a recombination expression carrier carrying the DNA sequence for encoding the protein. The protein is located in the top area of a mature sperm. A RT-PCR result shows that the gene is highly expressed in the epididymis and testis. A band of about 20 KD is detected in the corpus epididymidis part with Western blot. The HEL-89 protein can be used as a target protein for researching and developing immunity contraceptive as well as clinical diagnosis and treatment for male sterility. A method for detecting a corresponding gene or protein based on development of the HEL-89 protein can be widely used for the research field of reproductive medicine.
US7192970 Noncyclic 1,3-dicarbonyl compounds as dual PPAR agonists with potent antihyperglycemic and antihyperlipidemic activity Disclosed are the preparation and pharmaceutical use of novel noncyclic 1,3-dicarbonyl compounds of formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Y, Z, Q, Ar and n are as defined in the specification. These compounds, as peroxisome proliferator-activated receptor (PPAR) dual agonists for both RXR/PPARgamma and RXR/PPARalpha heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders
WO2012092485A1 Enhancement of placental stem cell potency using modulatory rna molecules Provided herein are methods of producing enhanced placental stem cells by modulatory RNA molecules. Also provided herein are methods of using enhanced placental stem cells, for example, to treat individuals having a disease, disorder or condition caused by, or relating to, an unwanted or harmful immune response. Further provided herein are compositions comprising said enhanced placental stem cells.
EP2624826A1 Vitamin e formulations of sulfamide ns3 inhibitors The invention relates to new formulations of compounds having activity against HCV- associated disorders, new combinations, new methods of treatment and their use in therapy.
CA2193337C 1-phenyl-2-dimethylaminomethyl-cyclohexan-1-ol compounds as pharmaceutical active ingredients 1-phenyl-2-dimethylaminomethyl-cyclohexan-1-ol compounds, methods of preparing them and the use of these compounds in drugs are described.
CN101259135B Antidiarrheal pharmaceutical composition for animals and preparation method thereof The invention discloses an antidiarrheal drug composition for livestock, which consists of the following ingredients by weight portion: 200-400 portions of amikacin sulfate, 15-25 portions of furosemide and 5-15 portions of dexamethasone. The preparation method of the antidiarrheal drug is that: firstly, a dexamethasone injection is mixed into an amikacin sulfate injection in the above ratio, andthen mixed with a furosemide injection and sealed into a bottle. The antidiarrheal drug composition of the invention has clear curative effect, good efficacy, rapid disappearance of diarrhea; diuresiseffect of the furosemide injection is utilized to absorb water and reduce intestinal water; the anti-inflammatory effect of dexamethasone is applied to mitigating clinic sympton; the antidiarrheal speed is accelerated and the pain of sick livestocks is relieved by the cooperation of these three medicines.
CN103239724A Anti-thrombosis combined drug and pharmaceutical composition thereof The invention provides the use of aspirin, dipyridamole, and proton pumps in preparing an anti-thrombosis combined drug, wherein the weight ratio of aspirin to dipyridamole to proton pumps is (0.5-4): (5-20): 1. The invention also provides a pharmaceutical composition. The anti-thrombosis combined drug is formed by combining aspirin, dipyridamole and proton pumps together, and thus superior to combined utilization of aspirin and dipyridamole in anti-thrombosis effect; and the anti-thrombosis combined drug is excellent in gastric mucosa protection effect, and thus achieves double effects of more effectively preventing thrombosis and reducing the side-effects of the gastrointestinal tract.
CN103070741A Application method of aluminum foil materials as warmer materials to external slimming drug The invention relates to an application method of aluminum foil materials as warmer materials to external slimming drug. The aluminum foil materials of OPP (oriented polypropylene)/VMPET (vacuum aluminum-plating polyethylene terephthalate)/LLDPE (linear low density polyethylene) through compounding. In the VMPET, a coating is arranged between an aluminum plating layer and PET (polyethylene terephthalate), and ventilation holes are distributed in the aluminum foil materials. The aluminum foil materials have the advantages that the coating is firstly coated on the surface of an aluminum plating base material PET film, and the vacuum aluminum plating is carried out, so the coating is arranged between the aluminum plating layer and the PET film and realizes the effect of a buffer layer, the damage to the aluminum plating layer is reduced, the coating is used as the warmer materials for improving the action effect of the external slimming drug, and the effect exerting of the slimming drug is promoted through an external heat source. The slimming drug adopted in the application method consists of 10 to 30g of Xiangfu, 10 to 30g of rhizoma alismatis, 10 to 30g of angelica sinensis, 10 to 30g of betel nut, 10 to 30g of borneol, 10 to 30g of star anise, 10 to 30g of rhizoma alismatis leaf and 10 to 30g of rhizoma atractylodis. When the external slimming drug is adopted to be smeared at the abdomen of the human body, drug ingredients are permeated into the skin of the human body under the effect that the aluminum foil materials provide heat sources, and the effects of enhancing the metabolism and promoting the microcirculation and fat absorption conversion are reached. The external slimming drug has the characteristics that the medicine use is convenient, the effect is obvious, no rebound is generated, and the food limitation is not needed. The external slimming drug is suitable for the application of subcutaneous fat reduction and weight reduction to patients.
WO2013064672A3 Oxazaphosphorines dosed one time for treating diseases The invention relates to oxazaphosphorines of formula (I), wherein R1 and R2 are 2-chloroethyl or H and R3 is 2-sulfonatoethylthio or H, for treating diseases that are caused or maintained by the tolerogen indolamine-2,3-dioxygenase (IDO), wherein the oxazaphosphorines of formula (I) are administered one time in a dose of at most 0.3 mmol/m2 and thus act against the tolerogen IDO. The invention further relates to the use of said oxazaphosphorines to produce a medication for use in treating diseases that are caused or maintained by the activation of the expression of indolamine-2,3-dioxygenase (IDO), wherein the oxazaphosphorines of formula (I) are administered one time in a dose of at most 0.3 mmol/m2.
US20070031374 Treating cell proliferative disorders via administration of mixture comprising interleukin-21 and anti-cancer monoclonal antibody The invention provides combination treatments with IL-21, analogues and derivatives thereof.
WO2013109514A1 New forms and salts of a dihydropyrrolo[1,2-c]imidazolyl aldosterone synthase or aromatase inhibitor The invention relates to a phosphate salt or a nitrate salt of 4-(R)-6,7- dihydro-5H-pyrrolo[l,2-c]imidazol-5-yl-3-fluoro-benzonitrile having following formula: especially in crystalline form, and specific forms of these salts, as well as related invention embodiments. The salts and salt forms allow for the prophylactic and/or therapeutic treatment of aldosterone synthase and/or aromatase mediated diseases or disorders such as Cushing's disease.
WO2013005216A1 Compositions and methods for treatment of renal ischemia-reperfusion injury The invention provides compositions and methods for prevention or treatment of renal ischemia-reperfusion injury using piperidine, pyrrolidine, or azepane derivatives comprising one to four nitric oxide donor groups and a reactive oxygen species (ROS) degradation catalyst.
WO2012033353A3 Sesterterpene compounds and use thereof The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed.
CN102846628A Application of veratryl fluorenol in preparing anti-ultraviolet compositions The invention provides an application of veratryl fluorenol 3 in preparing anti-ultraviolet compositions, and further provides an anti-ultraviolet composition which contains veratryl fluorenol 3 as an active component and one or more kinds of auxiliary materials suitable for external use of skins.
WO2006083019A1 AMYLOID β PROTEIN AGGREGATION INHIBITOR, DIAGNOSTIC AGENT FOR ABNORMALITY OF AMYLOID β PROTEIN, AND DIAGNOSTIC KIT FOR ABNORMALITY OF AMYLOID β PROTEIN Disclosed is an amyloid β protein aggregation inhibitor. The inhibitor comprises a compound represented by the chemical structure composed of a monosaccharide or a sugar chain having two or more monosaccharides, wherein a part or all of the OH groups are substituted by (i) a sulfo group or a salt of a sulfo group and (ii) a hydrophobic group and a part or all of the remainder of the substituted OH groups may be substituted by a group selected from H, NH2, NHR6 and NHR6R7. Particularly preferably, the inhibitor is a compound represented by the general formula (1).
US20120083531 Calcium citrate and calcium lactate formulations for alteration of biophysical properties of mucosal lining The present invention relates to pharmaceutical compositions suitable for inhalation, comprising as an active ingredient calcium lactate or calcium citrate. The invention also relates to methods of treating, preventing, and reducing the spread of an infection of the respiratory tract, comprising administering a pharmaceutical composition that comprises calcium lactate or calcium citrate as an active ingredient.
CN102813651A Pharmaceutical composition containing esomeprazole sodium, and preparation method thereof The invention relates to a pharmaceutical composition containing esomeprazole sodium, and a preparation method thereof. Among the active components of the pharmaceutical composition provided by the invention, the amount of 5-(-)-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfonyl]-1H-benzimidazole sodium is lower than 0.3%. The invention also provides a method for producing a target product through a salt forming reaction and recrystallization of esomeprazole. With the controlling over reaction conditions and reaction solvents, advantages such as simple process, low cost, high yield, and suitability for industrialized productions are realized, and the esomeprazole sodium provided by the invention can be obtained. The invention also provides prescriptions and a preparation method of the pharmaceutical composition.
CN101948429B 1-methyl-7H-indene[1, 2-b]quinolinetrifluoromesylate-7-(4-dimethylamino) benzyl alkene derivant and preparation thereof The invention belongs to the field of antitumor drug preparation, in particular to a 1-methyl-7H-indene[1, 2-b]quinolinetrifluoromesylate-7-(4-dimethylamino)benzyl alkene derivant used as a DNA topoisomerase inhibitor and a preparation method thereof. The preparation method comprises the following steps of: (1) salification reaction: reacting 7H-indene [1, 2-b]quinoline with methyl trifluoromethanesulfonate in the molar ratio of 1 to (2-3) under the protection of nitrogen gas at room temperature with stirring to obtain 7H-indene[1, 2-b]quinolinetrifluoromesylate; (2) coupling reaction: reacting the obtain 7H-indene[1, 2-b]quinolinetrifluoromesylate and 4-dimethylaminobenzaldehyde in the molar ratio of 1.0:(1.4-1.6) in glacial acetic acid in refluxing to prepare the 1-methyl-7H-indene[1, 2-b]quinolinetrifluoromesylate-7-(4-dimethylamino)benzyl alkene derivant. The prepared compound has strong inhibition action on leukemia cells and human laryngeal squamous carcinoma cells; moreover, the preparation method has the advantages of simple process and good yield reaching about 65%.
CN103145733A Amoxicillin compound and pharmaceutical composition of amoxicillin compound and potassium clavulanate The invention relates to an amoxicillin compound and a pharmaceutical composition of the amoxicillin compound and potassium clavulanate. The pharmaceutical composition is an oral sustained-release preparation. The amoxicillin compound is a crystalline compound which is provided with the following structural formula, wherein the characteristic peaks as shown in an X-ray powder diffraction pattern obtained by measuring through Cu-K alpha rays are displayed in 2 theta of 8.0 degrees, 12.1 degrees, 15.4 degrees, 17.0 degrees, 19.8 degrees, 21.6 degrees, 23.0 degrees, 24.3 degrees, 25.7 degrees, 27.4 degrees, 30.7 degrees and 33.5 degrees. The novel crystalline compound is improved in stability and dissolubility. The amoxicillin and clavulanate potassium prepared from the crystalline compound is higher in stability. The amoxicillin and clavulanate potassium oral sustained-release preparation prepared from the crystalline compound can be synchronously released, and is excellent in in-vitro dissolution and higher in bioavailability.
US20100168192 Benzisoxazole derivatives as potassium channel modulators for the treatment of e.g. respiratory diseases, epilepsy and convulsions This invention relates to novel benzisoxazole derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels e.g. a respiratory disease, epilepsy or convulsions. X represents a substituent selected from the group consisting of CO—NR′R″, CO—O—R′, CO—NH—S, CO—NH—SO2R″′, CO—NH—C═N, SO2—NR′R″, 2,3-dihydro-1-H-tetrazol-5-yl and [1,2,4]oxadiazolidin-5-one; wherein R′ and R″, independently of each other, represent hydrogen or alkyl or phenyl; and R″′ represents alkyl, cycloalkyl, haloalkyl or phenyl, which phenyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, trifluoromethoxy, cyano and nitro.
CN101721453A Composition for deferring male senility and preparation method thereof The invention discloses a composition for deferring male senility and a preparation method thereof. The composition is prepared from ginseng, fiveleaf gynostemma herb, Chinese caterpillar fungus solid fermentation powder and vitamin C according to a certain weight proportion. The composition can be prepared into any one of common formulations. The composition has the effects of tonifying Qi, keeping strong, reducing blood pressure, reducing blood fat and removing free radicals, is particularly suitable for elderly and middle-aged men to take, and can defer senility and promote health.
CN101647885B Medicine composition for treating coughs The invention relates to a medicine composition for treating coughs, which consists of active medicine ingredients and adjuvant material ingredients acceptable in medicaments, wherein the active medicine ingredients comprise the following raw materials in proportion by weight: 120-480 parts of bitter almond, 120-480 parts of liquorice, 35-150 parts of radish seed, 35-150 parts of balloon flower and 35-150 parts of plaster. The medicament has the efficacy of freeing lung and clearing heat, relieving coughs and reducing sputum, relieving asthma and the like, and can be used for treating diseases including respiratory tract infection, tracheitis, pneumonia, coughs and the like.
CN101108174A Pharmaceutical composition having active ingredient of tamsulosin hydrochloride and finasteride The invention relates to a drug compound that takes tamsulosin hydrochloride and finasteride as its active ingredients as well as its preparation method and purpose. The invention, which takes tamsulosin hydrochloride and finasteride as its active ingredients and forms drug compound by mixing pharmaceutically acceptable supplementary materials, can be applied for the treatment of benign hyperplasia of prostate. The invention takes tamsulosin hydrochloride and finasteride as its active ingredients and adds the supplementary materials with certain portion and sorts, then develop them into tablet, capsule, dispersible tablet, chewable tablet, toroches and pill via the preparation technology in the invention.
US7019004 Agonists of imidazolidine-2,4-dione derivatives, chemical intermediates, for treating anxiety, depression, schizophrenia, neurodegenerative diseases, dementia, epilepsy, endocrinological disorders associated with excess of hormone, tumor The invention provides compounds of formula (I) wherein X, Y, R1, R2, R3 and R4 are as defined in the description, and the preparation thereof. The compounds of the formula bind to somatostatin receptors and are useful as pharmaceuticals
US8158619 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl compounds and their medical use This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
US20080261986 Pharmaceutical formulations for iontophoretic delivery of an anti-fungal drug Pharmaceutical formulations suitable for iontophoresis thereof that provide enhanced iontophoretic delivery of an anti-fungal drug to at least one body surface are described. Also described are pharmaceutical formulations suitable for iontophoresis comprising terbinafine and methods for administering terbinafine to a body surface via iontophoresis. In one embodiment, the body surface includes a nail plate and/or the skin.
US20090143379 Storage stable perfusion solution for dihydropteridinones Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and in the specification, and an amount of a physiologically acceptable acid or mixture of acids sufficient to dissolve the active substance and act as a stabiliser, optionally together with other formulating excipients suitable for parenteral administration, and a process for preparing the infusible or injectable solutions according to the invention.
US20110207791 Composition of a 5-ht2a serotonin receptor modulator useful for the treatment of disorders related thereto The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.
WO2012007868A3 N- sulfonylbenzamides as inhibitors of voltage - gated sodium channels The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
CN101057925B Preparation technology for 'jieguqili' capsule The invention relates to a process for preparing bone-fixation capsules and its quality control method, wherein the preparing process consists of disintegrating olibanum, myrrh and Chinese angelica root into coarse powder, extracting volatile oil with aqueous vapor, coating with volatile fluid, disintegrating dragon's blood resin and borax into fines, grilling drynaria, native copper and rheum officinale with water, merging grilling liquid with distilled aqueous solution, filtering, concentrating, charging volatile oil inclusion compound, dragon's blood resin, borax fines and right amount of adjuvant.
CN102626105A Iodic acid disinfectant The invention belongs to the technical field of chemical disinfectants, in particular to an iodic acid disinfectant which is used for disinfecting surgical operation positions, livestock houses, animal product processing places and utensils. The iodic acid disinfectant is prepared by 1.80%-2.50% of potassium iodide, 1.35%-1.50% of refined iodine, 16.0%-17.0% of 85% phosphoric acid, 0.18%-0.28% of 98% concentrated sulfuric acid, 15.00%-25.00% of absolute ethyl alcohol, 0.04%-0.10% of sodium dodecyl benzene sulfonate and the balance water. The prepared iodic acid disinfectant can exert the disinfecting and sterilizing effect well and quickly kill various bacterium propagule, bacterial spore, virus, fungus, mycoplasma and the like in livestock farms.
CN102114114A Nursing disinfectant and preparation method thereof The invention relates to a nursing disinfectant and a preparation method thereof. The nursing disinfectant mainly comprises the following ingredients: guang musk, gardenia, manuka, orange oil, phellodendron, frankincense, peppermint oil, angelica dahurica, lightyellow sophora root, jasmine essence, nidus vespae, eucalyptus oil, juniper berry and the like. The nursing disinfectant can effectively kill bacteria on human skin, and has the effects of reducing inflammation, relieving pain, promoting blood circulation, removing blood stasis, accelerating wound healing, and repairing human surface skin.
WO2008077614A2 Use of a composition made of mineral nutrients and optionally acetogenic and/or butyrogenic bacteria in order to avoid or reduce the formation of gas in the large intestine of a mammal and the resulting abdominal problems The present invention relates to a composition, comprising one or more mineral nutrients selected from the group consisting of selenium, molybdenum, or tungsten, which are galenically or chemically configured such that the mineral nutrient or the mineral nutrients are completely or partially released only shortly before, upon, or shortly after reaching the large intestine. The invention further relates to the use thereof for producing a pharmaceutical product for administration in a mammal in order to avoid or reduce the formation of gas in the large intestine and the resulting abdominal problems, particularly flatulence, meteorism, or abdominal cramps. Furthermore, the invention relates to a method for isolating acetogenic and butyrogenic bacteria strains, which are suited for the above therapeutic purposes.
WO2010151784A2 Antimicrobial compounds This disclosure relates to compositions including certain compounds identified by a quantitative, high throughput assay to be effective in inhibiting the ability of a bacterium to kill a host organism, as well as methods for using these compounds for treating bacterial infections.
US20050203113 Compounds and method for the treatment of overactive bladder NK2R binding compounds in accord with structural diagram I useful for the treatment or prevention of OAB or UI in mammals, particularly humans are disclosed: wherein in said compounds D, A, R1, R3 and R4 are as defined in the specification. Pharmaceutically-advantageous salts of the compounds, methods of use of the compounds, either alone or in combination with other pharmacological agents, and pharmaceutical compositions useful in practicing the methods of the invention are also disclosed.
CN103371986A Application of urushiol compound to preparation of drug for inhibiting fibering of liver tissue The invention provides application of a urushiol compound to preparation of a drug for inhibiting fibering of liver tissue, and particularly provides a urushiol compound shown in the structural formula 1 and application of medical salt of the urushiol compound in preparation of a drug for inhibiting fibering of liver tissue. The urushiol compound provided by the invention has a good effect of inhibiting the fibering of liver tissue and is free of fatal toxic and side effects. The urushiol compound and the medical salt provided by the invention can be prepared into an oral agent or an injection type medicinal preparation for inhibiting the fibering of liver tissue.
WO2014021464A1 Hydroxylated krn7000 analogue and use thereof The purpose of the present invention is to provide: a novel KRN7000 analogue which is expected to have an immunosuppressive effect and is biased toward type-Th2;and a medicinal agent comprising the KRN7000 analogue. A compound represented by formula (I) (wherein R1 represents a hydrogen atom or a hydroxy group; two R2's may be the same as or different from each other and independently represent a hydrogen atom or a hydroxy group; R3 represents a hydrocarbon group having 8 to 14 carbon atoms which may have a substituent; and R4 represents a hydrocarbon group having 18 to 24 carbon atoms which may have a substituent) or a salt thereof.
US20110009435 Hetero bicyclic carboxamide derivatives and their pharmaceutical use and compositions The present invention relates to compounds of Formula I and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.
CN101328123A 5-oxo-substituted benzene acryloyl quinate methyl ester compound and use thereof The invention provides a 5-oxygen-substituted benzene ethylenic propionyl quinic acid methyl compound and an officinal salt (I) thereof as well as an important intermediate of 5-oxygen-[3-substituted benzene ethylenic propionyl]-3, 4-acetone fork quinic acid methyl ester compound for preparing the compound (I) and an officinal salt (II) thereof. The compound (I) and the compound (II) have the functions of restraining DNA of hepatitis b virus from copying and reducing the expression of a surface antigen of the hepatitis b virus and can be applied to prepare a medicine for treating hepatitis b virus infectious diseases. The structural formulas of the compound (I) and the compound (II) are shown above.
WO2010107069A1 Amino acid-containing ophthalmic composition Disclosed is an ophthalmic composition which is useful for prevention or treatment of dry eye conditions, especially for prevention or treatment of dry eye conditions associated with serious epithelial disorders. Specifically disclosed is an ophthalmic composition which is characterized by containing at least one amino acid selected from a group consisting of alanine, asparagine, glutamine and arginine. The ophthalmic composition preferably contains: two or three amino acids selected from among alanine, asparagine and glutamine; three amino acids, namely arginine, asparagine and glutamine; or two amino acids, namely arginine and glutamine. Also disclosed is an ophthalmic composition for prevention or treatment of ocular surface disorders, especially for prevention or treatment of corneal and conjunctival epithelial disorders.
US20090228997 Extracellular novel RAGE binding protein ( EN-RAGE) and uses thereof The present invention provides for an isolated human EN-RAGE peptide. The present invention also provides for a method for determining whether a compound is capable of inhibiting the interaction of an EN-RAGE peptide with a RAGE peptide, which comprises: (a) admixing: (i) a RAGE peptide or an sRAGE peptide or a fragment of either thereof, (ii) an EN-RAGE peptide or a fragment thereof, and (iii) the compound; (b) measuring the level of interaction between the peptide of step (a) (i) and the peptide of step (a) (ii), and (c) comparing the amount of interaction measured in step (b) with the amount measured between the petpide of step (a)(i) and the peptide of step (a) (ii) in the absence of the compound, thereby determining whether the compound is capable of inhibiting the interaction of the EN-RAGE peptide with the RAGE peptide, wherein a reduction in the amount of interaction in the presence of the compound indicates that the compound is capable of inhibiting the interaction. The present invention also provides for a method for inhibiting inflammation in a subject which comprises administering to the subject a compound capable of interfering with the interaction between EN-RAGE peptide and receptor for advanced glycation endproduct (RAGE) in the subject thereby inhibiting inflammation in the subject.
CN102973549A Drug composition The invention belongs to the technical field of medicine, and provides a drug composition, which comprises germacrone, furanodiene, curdione, beta-elemene, curcumenol, curzerene and borneol. The drug composition has characteristics of definite components and controllable quality. With the drug composition, weights of curcumenol and curzerene are controlled so as to reduce drug irritation. The drug composition can be adopted for preparing suppositories, ointments, capsules, effervescent tablets, gelatas, lotions, pellicles or foam agents, provides good treatment effects for HR-HPV and/or LR-HPV and cervical diseases, and is suitable for wide clinical applications.
EP1560827B1 Anti-infective agents The present invention provides an HCV polymerase inhibiting compound having the formula (I) and a composition comprising a therapeutically effective amount of said compound. The present invention also provides a method for inhibiting hepatitis C virus (HCV) polymerase, a method for inhibiting HCV viral replication, and a method for treating or preventing HCV infection. Processes for making said compounds, and synthetic intermediates employed in said processes, are also provided.
EP2303184A1 Combination treatment of glaucoma The methods described herein provide reduction of intraocular pressure by administering a sustained release formulation including latanoprost and a pharmaceutically acceptable vehicle and administering an eye drop adjunctive composition to the eye of a patient. The sustained release formulation can release latanoprost continuously for at least 90 days from a punctum plug delivery system. The eye drop adjunctive composition can also include latanoprost.
US20090270501 Composition and method for increasing the anabolic state of muscle cells A nutritional supplement comprising at least a therapeutically effective amount of ethyl pyruvate and a therapeutically effective amount of at least one α-hydroxy branched-chain amino acid metabolite is provided by the present invention. The ingredients of the present nutritional supplement substantially simultaneously act to induce a anabolically-favorable state for muscle by substantially simultaneously maintaining blood and muscle physiological pH levels as well as increasing cellular concentrations of branched-chain amino acids. Both a composition and a method are provided by the present disclosure.
CN103083310A Application of luteolin in preparation of ovarian senescence resistance medicines The invention discloses application of luteolin in preparation of ovarian senescence resistance medicines. The luteolin has obvious effects in treatment of multiple ovarian regression diseases such as polycystic ovarian syndrome, dysfunctional uterine bleeding, premature ovary failure or climacteric syndrome. The luteolin is prepared into oral medicines, transdermal delivery medicines or injection medicines for treating the ovarian regression diseases.
CN101518512A Calcium gluconate injection and preparation method thereof The invention discloses a calcium gluconate injection, each liter of which contains 90 to 110g of calcium gluconate, 5 to 9g of lactic acid, 0.2 to 0.5g of calcium hydroxide, 9 to 11g of sodium hydroxide, 0.5 to 5g of sodium gluconate and the balance water for injection. The calcium gluconate injection is prepared according to the following steps: taking and boiling the water for injection; adding and stirring calcium gluconate to the water to dissolve; adding sodium gluconate, calcium hydroxide and lactic acid in turn; heating the mixture to boil and stirring to dissolve; adding the sodium hydroxide solution for adjusting the pH value; adding activated carbon; stirring the activated carbon evenly; standing and filtering the resultant ; adding the full quality of water for injection to the resultant; finely filtering the resultant to qualify; and encapsulating and sterilizing the resultant under high pressure. The calcium gluconate injection has strong stability and stable quality, and basically does not generate crystals within the storage period at low temperature.
US20120095058 Method of preventing survival of retrovirally cells and of inhibiting formation of infectious retroviruses The present invention discloses compounds and pharmaceutical compositions which are highly effective at inhibiting the accumulation of spliced and unspliced viral transcripts and their utilization for viral protein synthesis at cellular ribosomes, and at inhibiting the formation of the hypusine residue in cellular eIF-5A precursor proteins, the cellular cofactors that render spliced and unspliced viral transcripts translatable at the ribosomes of infectled cells. The invention further relates to methods of using such compounds and pharmaceutical compositions therefrom for inhibiting or preventing viral protein synthesis. Such inhibition cause a dose-dependent release from the virally induced arrest of the otherwise genetically preprogrammed apoptosis of virally infected cells, and in consequence, triggers their apoptotic ablation and the eradication of the chronic infection-mediating provirus integrated into their genome.
US20070238638 Bak promoter expression system The present invention provides polynucleotides which regulate the expression of a gene involved in apoptosis. Also provided are methods for identifying agents that modulate expression of a gene involved in apoptosis.
WO2007070701A3 Compositions and methods for preserving brain function Compositions and methods for preventing, reducing, or delaying decline in one or more of cognitive function, motor function, cerebrovascular function, or behavior in animals, particularly geriatric animals, are disclosed. The compositions and methods utilize medium chain triglycerides.
WO2007067966A1 Method and formula for prevention of cold and flu and suppression of related symptoms The present invention generally relates to methods, compositions and systems for preventing the common cold and flu, for reducing the duration of common colds and flu, for reducing the severity of common cold and flu symptoms and for reducing/eliminating the transmission of the common cold and flu. Specifically, it relates to the treatment a of subject having a cold with a composition comprising cesium and/or rubidium ions. In a composition aspect, the present invention provides a composition for treating a common cold and flu.
WO2006129881A1 Prophylactic/therapeutic agent for bone/joint disease and screening method for the agent Disclosed is a regulator of the differentiation of an osteoblast or chondrocyte or a prophylactic or therapeutic agent for a bone/joint disease which has a novel mechanism of action. More specifically, disclosed are: a regulator of the differentiation of an osteoblast or chondrocyte or a prophylactic or therapeutic agent for a bone/joint disease which comprises a substance capable of regulating the expression or function of nrf2; a method for screening a substance capable of regulating the differentiation of an osteoblast or chondrocyte or a substance capable of preventing or treating a bone/joint disease, the method comprising the step of determining whether or not a substance to be tested can regulate the expression or function of nrf2; a method for identification of an nrf2 mutation which causes any change in the differentiation of an osteoblast or chondrocyte; a diagnostic agent for a biological condition of an animal with respect to the differentiation of an osteoblast or chondrocyte; a diagnostic agent for the differentiation efficiency of an osteoblast or chondrocyte; an osteoblast or chondrocyte in which the expression of nrf2 is regulated; and others.
CN1732978A Externally applied medicine for treating vitiligo and its preparation process The invention relates to an externally applied medicine for treating vitiligo and its preparation process, wherein the externally used medicament is prepared from acetic acid, 2-hydroxybenzoic acid, bluestone, ferrous sulfate and iron rust through immersion.
EP1858517A2 Pharmaceutical compositions for the treatment and/or prevention of schizophrenia and related diseases The invention relates to new pharmaceutical compositions for the treatment and/or prevention of schizophrenia and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibandserin as one active ingredient in combination with at least one additional active ingredient for the treatment and/or prevention of schizophrenia and methods for the preparation thereof.
DE102009034131A1 Composition, useful e.g. as volume substitute, and for prophylaxis and therapy of reperfusion syndrome and hypovolemia, comprises an aqueous composition of inosine and a hydrocolloid including hydroxyethyl starch, gelatin and/or albumin Pharmaceutical composition (I) comprises an aqueous composition of inosine and at least one hydrocolloid including hydroxyethyl starch, gelatin or its derivatives and/or albumin or its derivatives. - ACTIVITY : Vasotropic. - MECHANISM OF ACTION : None given.
US7393834 LHRH-antagonists in the treatment of fertility disorders A method of treating infertility disorders by 1) administering an LH-RH antagonist, preferably Cetrorelix, in amounts to selectively suppress endogenous LH but not FSH secretion and 2) inducing follicle growth by administration of exogenous gonadotropin. The selective suppression OF LH allows FSH secretion to be at natural levelS thereby not affecting individual estrogen development. The LH-RH antagonist can be given as a single or dual subcutaneous dose in the range of 1 mg to 10 mg, preferably 2 mg-6 mg. In multiple dosing-posology, LH-RH antagonist can be administered subcutaneously in an amount in the range of 0.1 to 0.5 mg of LH-RH antagonist/day. LH-RH antagonist is applied starting cycle day 1 to 10, preferably on day 4 to 8, and ovulation can be induced between day 9 and 20 of the menstruation cycle by administering rec. LH, native LH-RH, LH-RH agonist or by HCG. In addition rec. LH, native LH-RH or LH-RH agonist can be given to avoid hyperstimulation syndrome and native LH-RH or a LH-RH agonist can be administered to avoid luteal phase stimulation by neutralizing the negative effects of HCG.
WO2005097783A8 Thiocarbamoylprolines The invention relates to novel compounds of formula (I) wherein R, R1, R2, R3 and R4 have the meaning cited in claim 1, inhibit coagulation factors Xa and can be used in the prophylaxis and/or therapy of thromboembolic diseases and for treating tumours.
WO2012156936A1 Substituted indole derivatives for the treatment of immunological disorders The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. (I).
WO2006108358A1 ANTIVIRAL USE OF ARTIFICIAL CpG-CONTAINING SINGLE-STRANDED OLIGODEOXYNUCLEOTIDES IN COMBINATION WITH RIBAVIRIN The present invention provides a composition containing ribavirin and artificial CpG single-stranded oligodeoxynucleotides or a kit which can prevent or treat viral infection and infectious diseases caused by virus, and use thereof. The invention also provides a method for preventing or treating viral infection and infectious diseases caused by virus.
US7803805 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl)-3-oxo-propionitrile mono citrate salt; immunosuppressants, autoimmune diseases, skin disorders, Crohn's disease, antidiabetic agents, anticancer agents, antiarthritic agents This invention relates to novel amorphous and crystallline forms of 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3 -oxo-propionitrile mono citrate salt, useful as inhibitors of protein kinases, and to their methods of preparation.
US20080249146 Bicyclic antivirals for hepatitis C treatment; e.g. 1-cyclohexyl-2-phenyl-1H-thieno[3,2-d]imidazole-5-carboxylic acid The present invention relates to compounds of the formula (I), wherein R1, R2, A, B, D, E, F, G and Ar are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
US20080194639 Proton Pump Inhibitors in the Treatment of Sleep Disturbance Due to Silent Gastroesophageal Reflux The present invention relates to a new method of treatment of sleep disturbance due to silent gastro-esophageal reflux. In particular, the present invention relates to the use of certain proton pump inhibitors (PPIs) in said treatment.
CA2222279C Hypoxia inducible factor-1 and method of use The purified and characterization of hypoxia-inducible factor 1 (HIF-1) is described. HIF-1 is composed of subunits HIF-1.alpha. and HIF-1.beta.. Purified HIF-1.alpha. polypeptide, its amino acid sequence and polynucleotide sequence are provided. A HIF-1.alpha. variant that dimerizes to HIF-1.beta. producing a nonfunctional HIF-1 complex is described. Methods for the prevention and treatment of hypoxia-related disorders are provided.
US20120003305 Oral Dosage Forms Of Bendamustine In the present invention there is provided an oral pharmaceutical composition, comprising bendamustine or a pharmaceutically acceptable, ester, salt or solvate thereof as an active ingredient, and a pharmaceutically acceptable excipient, which is a pharmaceutically acceptable non-ionic surfactant, selected from the group consisting of polyethoxylated castor oil or derivative thereof and a block copolymer of ethylene oxide and propylene oxide.
WO2009126556A1 Pan-selectin inhibitor with enhanced pharmacokinetic activity Compounds, compositions and methods are provided for treatment of diseases or complications associated therewith, in which a selectin plays a role. More specifically, particular glycomimetics and uses thereof are described. For example, use of particular glycomimetics for treating sickle cell disease or a cancer involving a selectin, or complications associated with either, is described.
CN101669917A Scopolamine hydrobromide orally disintegrating microencapsule tablets based on NIMS system The invention relates to the technical field of medicines, particularly to scopolamine hydrobromide orally disintegrating microencapsule tablets based on a NiMS system and a preparation method thereof. The orally disintegrating microencapsule tablet provided by the invention is prepared by the NiMS system containing scopolamine hydrobromide and auxiliary materials. The auxiliary materials comprise microcrystalline cellulose, sodium carboxymethyl starch, mannitol, lactose, xylitol, magnesium stearate, superfine silica powder, etc. The copolamine hydrobromide orally disintegrating microencapsule tablet provided by the invention can be taken conveniently, and disintegrated rapidly in mouth by solvent of saliva without needing to drink water. The NiMS system further has a slow release effect,thereby not causing abnormal high blood drug concentration, reducing drug side effects, reducing local stimulation, and meeting requirements for special conditions and special groups, particularly the aged, children and patients who swallow difficultly.
WO2011063233A1 Amino heteroaryl compounds as beta-secretase modulators and methods of use The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein ring A, B1, B2, B3, L, R1, R4, R5 and m of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
EP2087885A1 Use of urokinase inhibitors for the treatment and /or prevention of neuropathological diseases The present invention relates to methods and compositions for the treatment and/or prevention of neuropathological and/or neurodegenerative diseases. In particular, the invention delivers novel uses of inhibitors of Urokinase-type Plasminogen activator in the treatment of amyotrophic lateral sclerosis.
US20100021484 Compositions, Methods and Kits Relating to Poxvirus Subunit Vaccines The invention is directed to a poxvirus vaccine comprising a soluble truncated poxvirus envelope protein. The invention is also directed to a vaccine comprising a nucleic acid encoding such proteins. Also included is an antibody which specifically binds to the proteins and nucleic acid encoding the same, as well as methods of preventing and treating a poxvirus infection using the afore-mentioned vaccine, antibody, protein, and nucleic acid encoding them.
US20080020018 Combination Products A pharmaceutical formulation comprises a plurality of seamless minicapsules having a diameter of from 0.5 mm to 5 mm, at least some of the minicapsules containing a methyxanthine as one active ingredient, and at least some of the minicapsules containing a corticosteriod as another active ingredient.
WO2011056764A1 Isotopically enriched or fluorinated imidazo[2,1-b][1,3]benzothiazoles Provided herein are isotopically enriched or fluorinated imidazo[2,1- b][1,3]benzothiazoles, for example, of Formula (I). Also provided are pharmaceutical compositions comprising such compounds, and methods of their use for the treatment of a proliferative disease.
EP1352650B1 Inhibitors against the production and release of inflammatory cytokines Medicines having inhibitory activity against the activation of NF-kB, which contain as the active ingredient compounds represented by the general formula (I)(wherein X is a connecting group; A is hydrogen or acetyl; E is aryl or heteroaryl; and Z is arene or heteroarene) or pharmacologically acceptable salts thereof: (I)
EP1928843A1 Bis-aryl urea compounds for the treatment of protein kinase-mediated diseaes The present invention relates to compounds of Formulas (I) and (II), wherein A1, A2, B1, B2, Q, X1, X2, Y and R3 are defined herein, synthetic intermediates, and pharmaceutical compositions, comprising such compounds. The compounds and compositions are capable of modulating various protein kinase receptors such as Tie-2 and, therefore, influencing kinase related disease states and conditions. The compounds, for example, are capable of treating cancer caused by unregulated angiogenesis, and inflammation as well as other proliferative disorders.
WO2009141573A1 Novel polymorph of tegaserod adipate The present invention relates to a novel crystalline form of tegaserod adipate and to processes for preparing said form. The invention also relates to pharmaceutical compositions comprising said crystalline form and to the use of said compositions in the treatment of gastrointestinal disorders, in particular irritable bowel syndrome.
WO2010011316A1 SUBSTITUTED 1,2,3,4- TETRAHYDROCYCLOPENTA[b]INDOL-3-YL) ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
US20120083533 Use of amides of mono- and dicarboxylic acids in the treatment of renal diseases A therapy for renal diseases, in particular renal diseases which develop in diabetic patients or patients who have been subjected to a treatment with an antitumor chemotherapy such as a platinum derivative and more generally cytotoxic drugs at renal level for treating of neoplastic diseases. More particularly, the present invention relates to palmitoylethanolamide and diethanolamide of fumaric acid for use in the treatment of renal diseases, in particular those caused by dysmetabolic diseases or by toxic or chemotherapy agents, such as platinum derivatives. Palmitoylethanolamide is used preferably in micronized or ultra-micronized form. Diethanolamide of fumaric acid is used preferably in aqueous solution.
EP1501795A1 Cinnamic acid amides The invention relates to compounds, methods for the production thereof, pharmaceutical compositions containing said compounds and the use thereof in the treatment and/or prophylaxis of diseases, especially bacterial diseases, in human beings and animals.
US20120184570 Theophylline Derivative Inhibits Osteoporosis The theophylline derivative disclosed in the present invention is characterized by having the pharmaceutical functions of osteoporosis. The theophylline derivative protects against bone resorption and inflammatory mediator infiltration.
US8138164 HCV NS3 protease inhibitors The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
US20080051365 Treatment of Inflammation The present invention concerns the therapeutic treatment of inflammatory conditions by a combined administration of methotrexate and an agonist of the A3 adenosine receptor. Provided are methods of therapeutic treatment comprising such a combined administration, pharmaceutical compositions useful in such methods comprising either an and use if either an agonist of the A3 adenosine receptor or methotrexate, as well as used of any of these active agents for preparing such a pharmaceutical composition.
CN102552189A Preparation method of simethicone drop pill The invention relates to the technical field of medicine, in particular to a preparation method of a simethicone drop pill which takes gelatin glycerin as a substrate. The method comprises the following steps of: (1) preparing a simethicone emulsion: mixing gelatin and purified water in the ratio of 1:(1.5-1.8), and soaking overnight; putting the gelatin which is soaked overnight into a melt tank, and heating to 55-65 DEG C till the gelatin is molten into a transparent liquid; and heating the simethicone to 60 DEG C, slowly pouring into a gelatin solution, and stirring for 2-3 hours till a mixture is completely emulsified; and (2) adding an appropriate amount of glycerin, a preservative and a pigment into the simethicone emulsion, stirring for about 1 hour, mixing uniformly, and conveying to a drop pill making machine with an appropriate method for making pills. According to the preparation method disclosed by the invention, simethicone contained in the simethicone drop pill can be completely emulsified, and the anti-foaming capability of the simethicone is brought into play; and moreover, the method has a simple process, is easy to control, and is suitable for industrial production.
CN102133204A Preparation method of melbinum osmotic pump controlled release tablets The invention relates to a preparation method of melbinum osmotic pump controlled release tablets for treating type 2 diabetes. The preparation method comprises the steps of preparing tablet cores, coating semi-permeable membrane layers, perforating, drying and coating damp-proof layers, characterized in that when the tablet cores are prepared, a medicinal salt of melbinum and a nonionic surfactant are added, and the nonionic surfactant accounts for 2-20wt.% of the medicinal salt of melbinum. The medicament disclosed by the invention has stable release, no irritation on intestinal tracts and few times of administration, is acceptable by patients, and greatly improves the compliance of patients.
WO2006136442A1 Pyrimidine derivatives for the treatment op gaba b mediated nervous system disorders The invention relates to novel heterocyclic compounds of the formula (I) in free base form or in acid addition salt form, in which R1, R2, R3, R4 and A are as defined in the specification, to their preparation, to their use as medicaments for the treatment of certain nervous system disorders and to medicaments comprising them.
CN101029022B Process for the preparation of 4-phenoxy quinoline derivatives The present invention provides a method for producing a chemical compound denoted in a general formula (a-11) or a salt or hydrate of the chemical compound that is acceptable pharmacologically, wherein, the producing method is to force a chemical compound denoted in the following general formula (a-12) to react with a chemical compound denoted in the following general formula (a-4).
US20100305105 Phenylsulfoxyoxazole compound inhibitors of urea transporters Provided herein are small molecule compounds that alter the transport activity of solute transporters, particularly urea transporters. The compounds described herein belong to the phenylsulfoxyoxazole, phenylsulfoxyimidazole, phenylsulfoxythiazole class of compounds. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating cardiovascular, renal, and metabolic diseases, disorders, and conditions. Methods for identifying and using these agents that inhibit urea transporters are described herein.
EP2131841B1 Methods for treating acute pain Methods of potentiating opioid-induced analgesia in a subject by administration of a phosphodiesterase (PDE) inhibitor or glial attenuator are described. In particular, the present invention is directed to methods of treating or preventing acute or subchronic pain by administration of a PDE inhibitor or glial attenuator, such as ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine), in combination with an opioid.
CN101011107A Pharmaceutical premixed agent for disease resistance and growth promotion and application thereof The invention relates to a method for preparing quinsadu premixed agent which can resist illness and accelerate the growth of animal. The inventive premixed agent comprises 5 deals of quinsadu and 95 deals of carrier, wherein, the carrier can be one or the combination of zeolite powder, talcum powder, calcium carbonate powder, degreased rice bran powder, corn powder or amidon. The inventive premixed agent can be used in the forage additive of pig, chicken, duck, fish, calf and lamb, while the relative contents are 25-100mg, 25-200mg, 25-100mg, 25-200mg, 25-150mg, and 25-100mg. The invention can accelerate the growth, reduce the forage cost and improve the animal quality, while it can control the infection of digestive canal.
US20120201824 Compositions and Methods for Inhibiting an Oncogenic Protein to Enhance Immunogenicity The present invention includes compositions and methods for inhibiting an oncogenic protein or its down-stream effector protein to suppress expression of a cell-surface protein involved in inhibiting immune response against malignant cells thereby enhancing immunogenicity of a cell. The invention includes inhibitors of expression of CD274 and/or its functional cell-membrane bound immunosuppressive analog. The invention includes inhibitors of function or expression of oncogenic ALK tyrosine kinase and/or other oncogenic proteins responsible for induction of expression of CD274 or its functional immunosuppressive equivalent. The invention includes inhibitors of function or expression of STAT3 and/or other cell signal transmitters and/or transcription factors activated by ALK or its functional analog involved in induction of expression of CD274 or its functional analog.
US20120203161 Deuterated water and riboflavin solution for extending singlet oxygen lifetimes in treatment of ocular tissue and method of use A solution of deuterated water containing a riboflavin-based photosensitizer is provided in order to extend life-times of UVA/Rf photo-generated intra-stromal singlet oxygen, in combination with UVA delivery profiles of pulsing, fractionation, and optionally auxiliary stromal/Rf hyper-oxygenation in order to accelerate protein cross-linking density rates in ocular tissue. A 100% deuterated water solution with 0.1% riboflavin in solution increases singlet oxygen lifetimes by at least an order of magnitude without inducing endothelial cell apoptosis, thereby also permitting use of some combination of lower percentages of deuterated water, lower concentrations of riboflavin or lower dosages of UVA on intact (un-debrided) epithelium for equivalent cross-link densities compared to current acceptable corneal cross-linking procedures. Lower concentrations of deuterated water with regular water, for example, yields shorter singlet oxygen lifetimes in approximately linear proportion to concentration, which are considered acceptable in therapies known or being developed in the art of corneal cross-linking.
WO2007113269A2 15-desmethoxymacbecin derivatives for the treatment of cancer diseases The present invention relates to 15-desmethoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and / or prophylaxis of cancer or B-cell malignancies.
CN103446142A Application of Lycojaponicumin C in pancreatic cancer treatment drug The invention discloses application of Lycojaponicumin C in preparation of a pancreatic cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Lycojaponicumin C also has remarkable inhabiting effect on growth of human pancreatic cancer cell strains PANC-1 and BXPC-3. Therefore, the Lycojaponicumin C can be used for preparation of an anti-pancreatic cancer drug and has good development and application prospect. The application of the Lycojaponicumin C in the preparation of the pancreatic cancer treatment drug is disclosed for the first time. Due to the fact that the fact that the skeleton type is a novel skeleton type, and the high pancreatic cancer cell inhibiting activity of the Lycojaponicumin C is previously unimagined.
WO2008123093A1 Agent for prevention or treatment of iron overload Disclosed is an agent for prevention or treatment of iron overload, which contains 22β-methoxyolean-12-ene-3β,24(4β)-diol or a pharmacologically acceptable salt thereof.
WO2007108727A1 Method for monitoring the effect of compounds on foxc2 expression The present invention relates to a method for monitoring/detecting compounds capable to regulate the transcription and/or expression of the forkhead transcription factor Foxc2, which compounds may be useful for the treatment of obesity related diseases and diabetes. The screening for the compounds has been performed in recombinant mouse cells containing the Foxc2 gene and the β-galactosidase gene in a suitable targeting vector.
WO2008108309A1 Fused pyridine derivative Disclosed is a fused pyridine derivative represented by the formula (I) below or a pharmacologically acceptable salt thereof. (In the formula, the symbols are as defined in the description.)
EP1112284B1 Piperazine-4-phenyl derivatives as inhibitors of the interaction between mdm2 and p53 A compound of formula (1), wherein: R5 is hydrogen, C1-4alkyl, R6CH2- or R6C(O)-; R6 is aryl, heteroaryl, heterocyclyl, aminoC3-6alkyl, N-(C1-4alkyl)aminoC3-6alkyl, NN-(diC1-4alkyl)aminoC3-6alkyl, or R7; wherein the aryl, heteroaryl or heterocyclyl rings may be optionally substituted with up to three substituents independently selected from nitro, C1-4alkyl, C1-4alkoxy, halo, (C1-4alkyl)sulfanyl, C1-4alkoxycarbonyl, N-(C1-4alkyl)carbamoyl, NN-(diC1-4alkyl)carbamoyl, N-(C1-4alkyl)amino or NN-(diC1-4alkyl)amino; wherein R7 is either a group or formula (2) or formula (3); and wherein L1, L2, L3, L4, R1, R2, R3, R4, R8, R9, R10, R11, R12, R13, A1, n, p, q, r and s are as defined in claim 1. The compounds of formula (1) inhibit the interactions between MDM2 and p53 and may be useful in the treatment of cancers.
US8367623 Glycolipid and medicine for autoimmune disease containing the same as active ingredient The invention is a glycolipid useful in treating autoimmune diseases and a medicine thereof as active ingredient for autoimmune diseases, represented by the formula wherein R1 is an aldopyranose group, R2 is a hydrogen atom or a hydroxyl group, R3 is —CH2—, —CH(OH)—CH2— or —CH═CH—, R4 is a hydrogen atom or CH3, x is 0-35, y and z represent integers satisfying y+z=0-3.
WO2014066695A1 Compositions and methods for treating estrogen-related medical disorders Disclosed is a compound of formula (I). or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions including the compound of formula (I) and methods of using the compound of formula (I).
CN102091077A Preparation process of alpha-amyrin fine particle The invention relates to a preparation process of an alpha-amyrin fine particle, which uses the traditional supercritical fluid anti-solvent equipment. The preparation process of the alpha-amyrin fine particle comprises the following steps of: (1) preparing alpha-amyrin liquid; (2) feeding carbon dioxide; (3) crystallizing and separating out alpha-amyrin; and (4) detecting. The preparation process is suitable for alpha-amyrin raw materials, can prepare the ultrafine particles which are beneficial to the absorption of a human body and can enhance the solubility and the curative effect of the alpha-amyrin and reduce the use cost and the toxic side effect; and in addition, the alpha-amyrin ultrafine particle prepared by the process has unique clinical advantages.
US20080045515 To treat Alzheimer's disease; compounds with an additional fused ring containing an SO2 group; to suppress or attenuate the secretion of beta -amyloid; (4aSR,6RS,8aSR)-6-[(4-chlorophenyl)sulfonyl]-6-(2,5-difluorophenyl)-3-ethyloctahydro-1H-2,1,3-benzothiadiazine 2,2-dioxide; cyclization, alkylation Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
CN102613456A Xylo-oligosaccharide composition with lipase activity inhibition effect and application of xylo-oligosaccharide composition The invention provides a xylo-oligosaccharide composition with a lipase activity inhibition effect. The xylo-oligosaccharide composition comprises xylo-oligosaccharide and L-arabinose. The composition has greater lipase activity inhibition effect than the single xylo-oligosaccharide or L-arabinose. The cooperative effect can be realized when the proportion of the xylo-oligosaccharide to the L-arabinose is 1:99 to 99:1 in the composition, the inhibition rate is greater than the maximum inhibition rate of the single ingredients when the proportion of the xylo-oligosaccharide to the L-arabinose in the composition is 1:99 to 45:55, and in addition, the optimized proportion is 40:60. The invention also provides hypolipidemic medicine, food, pet food and health care products. The medicine, the food, the pet food and the health care products comprise the composition disclosed by the invention. The composition provided by the invention has the advantages that the resources of raw materials are wide, the raw materials are easy to obtain, the cost is low, the functions are various, and the targeting is specific when the composition is applied to hypolipidemic products.
CA2582294A1 Condensed tricyclic benzimidazoles for the treatment of gastrointestinal disorders The invention relates to condensed tricyclic benzimidazoles of formula (I), in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.
US20080261873 Growth-Hormone Secretagogues Disclosed are methods of treating a disorder of the stomach, intestine or duodenum in a human subject. The method includes administering to the subject, a pharmaceutical composition comprising a compound that increases gastrointestinal motility (e.g., by modulating myenteric nerve activity) and/or induces the secretion or production of growth hormone.
CN103224492A 14-aryl-ether andrographolide derivative and preparation method and application thereof The invention discloses a 14-aryl-ether andrographolide derivative and preparation method and application thereof, and the structure is shown in the formula (I). The compound, isomer or salt thereof can be applied to medicament for regulating nuclear receptor function or preparation of medicament for preventing or treating diseases related to nuclear receptor FXR.
US20050176705 5-Chloro-1-(3,5-dichloro-2-methoxy benzenesulfonyl)-4-piperazin-1-yl-1H-indole trifluoroacetic acid salt; 5-hydroxytryptamine (serotonin) HT6 receptor antagonists; antidepressant, anxiolytic agent, cognition activator; ADHD, Alzheimer's and Parkinson's disease, drug and nicotine abuse The invention relates to novel indole compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of various CNS disorders.
CA2245545C Vaccines against varicella zoster virus gene 63 product The present invention relates to compositions for the treatment or prevention of Zoster of individuals infected with Varicella Zoster virus (VZV), and to the prevention and treatment of Varicella infections. The compositions of the invention comprise the protein encoded by VZV gene 63 or an immunologically active derivative thereof. The invention further relates to compositions containing DNA or RNA corresponding to VZV gene 63.
WO2012148225A2 Sustained-release pharmaceutical composition comprising donepezil or pharmaceutically acceptable salt thereof having improved dissolution stability and method for manufacturing the same The present invention relates to a sustained-release formulation comprising donepezil or a pharmaceutically acceptable salt thereof. More particularly, the present invention relates to a sustained-release pharmaceutical composition comprising donepezil or a pharmaceutically acceptable salt thereof, and one or more sustained-release bases selected from the group consisting of polyvinyl acetate and fatty acid ester, and a preparation method thereof.
CN101584677A Trimebutine maleate sustained-release tablet The invention relates to a trimebutine maleate sustained-release tablet, which comprises the following compositions: 300 g of trimebutine maleate; 55 g of hydroxypropyl methylcellulose; 1.0 g of dihydroxysuccinic acid; 2g of silicon dioxide; 4 g of magnesium stearate; and proper amount (2.7%) of ethyl cellulose alcohol liquid. The advantages of the invention are as follows: the trimebutine maleate sustained-release tablet is simple in formulation, simple to produce, low in production cost, stable in performance, which can fully satify the requirement of medicine.
CN102580092A Regulation of ferroportin and application thereof The invention relates to regulation of ferroportin and an application thereof, in particular to regulation of ferroportin by regulating an NF-kB channel. The invention provides an application of a substance for regulating an NF-kB channel to preparation of a medicament for regulating ferroportin expression, and an application of the substance to preparation of a medicament for treating diseases directly or indirectly related to iron metabolism. The invention further relates to a method for regulating ferroportin expression and a method for sieving a medicament for regulating ferroportin expression or a medicament for treating diseases directly relevant to or indirectly relevant to iron metabolism by regulating the NF-kB channel.
CN103142948A Medicine for preventing and treating respiratory diseases, and its preparation method The invention provides a medicine for preventing and treating respiratory diseases, and its preparation method. The preparation method is characterized in that the method comprises the following steps: dissolving borneol and menthol in edible ethanol and edible acetate acid gracial, sequentially adding edible vinegar, edible propionic acid, edible acetic acid, medical hydrochloric acid, food-grade formic acid and water, uniformly stirring, uniformly mixing the obtained substance with a powdery mixture or a volatile oil mixture of Atractylodes lancea, mint, Leaf of Tasmanian Bluegum, Artemisia argyi, Folium Viticis Negundo, Herba Schizonepetae, Folium Perillae, leaf of Chimonanthus nitens Oliv., Cymbopogon distans, Herba Moslae, dahurian angelica root, Manchurian wildginger, ginger, dried orange peel, Wrinkled Gianthyssop, Ligusticum sinense and lavender, and filling the obtained material to a bottle to obtain the medicine.
WO2014160079A1 Microemulsion topical delivery platform Provided are pharmaceutical carriers suitable based on oil-in- water microemulsions and methods of making same. Also provided are pharmaceutical compositions comprising a carrier of the invention and a lipophilic active pharmaceutical ingredient (API), as well as methods for making same. The pharmaceutical compositions are particularly suitable for use in formulating lipophilic APIs for topical administration to the eye. Specifically included are pharmaceutical compositions comprising fenofibrate or fenofibric acid as API. Also provided is a method of treating a disease of the posterior segment of the eye. Also provided is a pharmaceutical composition comprising a compound represented by (Formula I) formulated for topical administration to the eye.
WO2014060962A1 Pemetrexed dipotassium formulations The present application provides pharmaceutical composition/s comprising pemetrexed dipotassium hydrate and its uses thereof. The invention also provides process for preparing lyophilized compositions of pemetrexed dipotassium hemiheptahydrate.
CN103330710A Ramosetron composition for injection The invention provides a ramosetron composition for injection, and relates to the technical field of medicines and medicine manufacturing. Main medicines of the composition are ramosetron and melatonin. The melatonin comprises a quick release part and a slow release part contained in cyclodextrin. The ramosetron composition for injection provided by the invention has the functions of improving the treatment effect of ranitidine, avoiding instability, fast distribution and elimination and the like of MT (Melatonin) caused by oral absorption, reducing the first pass effect of MT and reducing the dosage of ramosetron. Delivery design combining quick release and slow release meets the physiological secretion characteristic of MT, solves the problem of short half life of MT and improves the bioavailability of the product. The composition has a synergistic effect on treatment of CINV (Chemotherapy Induced Nausea And Vomiting) by ramosetron, and after the melatonin is combined with ramosetron, not only is the CINV treated, is the treatment effect of the ramosetron on the CINV improved and is the course of treatment shortened, but also the use level of the ramosetron and the side effect of the ramosetron are reduced, and the immunity of human body is improved. The melatonin in a certain concentration in human blood has the capability of effectively reducing melatonin of human body to the benefit of treatment of the CINV.
CN1732913A Propylgallate injection liquid with favorable stability and its preparation process The invention provides a propylgallate injection with good stability and its preparing process, wherein the injection is prepared by using right auxiliary solvent and charging anti-oxidant, the water-solubility problem of the propylgallate injection can also be solved. The injection is used for treating cardiovascular and cerebrovascular diseases.
CN101693010A Cefathiamidine prosoma liposome preparation The invention provides a cefathiamidine prosoma liposome preparation, which comprises the following ingredients by shares: 1 share of cefathiamidine, 3-20 shares of hydrogenated soya bean lecithin, 2-12 shares of poloxamer 188-, 0.5-10 shares of deoxysodium cholate and 1-30 shares of proppants. The invention further provides a preparation method and usage of prosoma liposome. The prosoma liposome of the invention has the advantages of high stability, high entrapping efficiency, even grain diameters, small side effects and the like.
WO2007092645A2 Novel hcv inhibitor combinations and methods Novel hepatitis C virus ('HCV') inhibitor combinations comprising an HCV protease inhibitor and HCV polymerase inhibitor, and optionally one or more biologically active agents, as well as uses of these combinations as HCV inhibitors and for treating hepatitis C and related disorders are disclosed.
CN101791291A Sevoflurane venous microemulsion and preparation method thereof The invention relates to a medicinal preparation and a preparation method thereof, in particular to a sevoflurane venous microemulsion and a preparation method thereof, and belongs to the technical field of medicaments. The sevoflurane venous microemulsion is prepared from sevoflurane, oil for injection and auxiliary materials such as emulsifying agent and the like by using the microemulsion preparation technology. The sevoflurane venous microemulsion is clear and transparent liquid, has light blue opalescence, and has Tyndall phenomenon; and the medicament-loading rate is 0.01 to 2.00 percent, the average grain diameter is 10 to 100 nanometers, and the pH is 4.5 to 9.5. On the one hand, the sevoflurane venous microemulsion improves the bioavailability and treatment effect of the sevoflurane by changing an administration route, and on the other hand, the venous microemulsion has targeting and can reduce the toxic or side effect of the medicament; and meanwhile, the volatility of the sevoflurane is reduced to be minimum due to the package of the microemulsion so as to reduce the acrimony of the sevoflurane, alleviate the pain of a patient during injection, make the patient accept easily and improve the administration compliance of the patient.
WO2005077366B1 Use of non-peptidic nk1 receptor antagonists for the production of apoptosis in tumour cells The invention relates to the use of substance P antagonists and, in particular, the use of non-peptidic NK1 receptor antagonists for the treatment of cancer and, more specifically, human melanoma, neuroblastoma, glioma, human Hodgkin's lymphoma KM-H2, lymphoblastic leukaemia, human rhabdomyosarcoma, human breast carcinoma, human Burkitt's lymphoma, human lung carcinoma, human Ewing's sarcoma, human glioma and human osteosarcoma.
WO2009142731A2 Niacin and nsaid combination therapy Provided are pharmaceutical compositions and methods for preventing or reducing niacin-induced flushing comprising an aspirin component and a niacin component having different release profiles. Also provided are methods and compositions for preventing or reducing niacin-induced flushing comprising niacin, aspirin and a lipid-lowering drug other than niacin.
US20100197584 Use of curcumin to block brain tumor formation in mice The present invention provides compositions and methods of using curcumin or curcumin derivatives or analogs to activate the pro-apoptotic enzymes caspase-3/7 in cancer cells. The present invention also provides formulations of curcumin or derivatives or analogs with increased solubility or improved bioavailability. The formulations may be administered to a subject such that high concentrations of therapeutically effective curcumin compounds resuit in the subject's bloodstream. The invention thus involves the use of curcumin or curcumin derivatives or analogs to diminish cancer cell growth, decrease tumor size, prevent tumor formation, and Curcumin Carrier to reduce or prevent cancer or tumor cell invasion or metastasis into a tissue, e.g., into the nervous System and especially the brain, of a subject. The instant invention may be used prophylactically to prevent tumor formation or metastasis, as a monotherapy to treat existing tumors, after surgery to prevent recurrence of tumors or in conjunction with conventional cancer therapies to improve patient prognosis and reduce side-effects.
WO2014084434A1 Composition for preventing and treating rotator cuff injury, containing cyanidin or delphinidin as active ingredient To prevent and treat a rotator cuff injury, the present invention provides a composition for preventing and treating a rotator cuff injury, containing cyanidin or delphinidin as an active ingredient.
CN1803127A Limonene drop pills oral medicine for treating biliary passage disease and its preparation process The invention discloses a limonene medicinal drop pill for treating biliary tract diseases, wherein the existing dosage types for the conventional limonene preparations are modified to obtain drop pills with the advantages of simple process for manufacturing, shorter disintegration time, quicker action, better pharmaceutical stability, and longer effective period.
CN1871001A Alkynes III The present invention is directed to novel compounds of formula 1, to a process, for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds. The novel compounds are useful in therapy, and in particular for the treatment 5 of gastroesophageal reflux disease (GERD).
US20080312281 G-Protein Coupled Receptor (Gpr116) Agonists and Use Thereof for Treating Obesity and Diabetes Compounds of formula (I), or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes.
WO2010019059A1 Veterinary preparation The preparation contains preferably up to 30% (especially 15-25%) by weight of methisoprinol. Methisoprinol is preferably dissolved in water. Another form is a solution of methisoprinol in polyhydric alcohol, where the alcohol is propylene glycol or sorbitol. The preparation also contains excipients and additional ingredients. Methisoprinol has also been proved effective against papillomas.
CN102093366A Bicyclo-amino pyrazol compound and application of bicycle-amino pyrazol compound in resisting coxsackie virus The invention provides a bicyclo-amino pyrazol derivative with good coxsackie virus-resisting activity and a pharmaceutical composition containing the compound. An experiment indicates that the derivative has the strong coxsackie virus-resisting activity and is helpful to be developed into clinically effective antiviral medicaments.
WO2009041449A1 Antiobesity agent It is intended to provide an antiobesity agent having an elevated safety and improved qualities by which obesity can be ameliorated or prevented. An antiobesity agent containing reduced coenzyme Q as the active ingredient; and a drug, a quasi drug, a food, a food with health claims, a food for specified health uses, a cosmetic, a drug for animals, a pet food or a feed containing the antiobesity agent. A method of controlling obesity which comprises administering the above antiobesity agent containing reduced coenzyme Q as the active ingredient to a subject to be treated.
CN103254279A Polypeptide conjugate of paclitaxel or docetaxel The present invention discloses a series of polypeptide conjugates of paclitaxel or docetaxel, wherein 2' site hydroxyl of paclitaxel or docetaxel is conjugated with amino of a polypeptide through different conjugation sequences. The invention further discloses a preparation method of the polypeptide conjugate, and an application of the polypeptide conjugate in drug preparation. The polypeptide conjugate has characteristics of excellent anticancer activity, excellent cancer cell selectivity and good water solubility.
CN101869631A Toxicant elimination medicament for eyes The invention discloses a toxicant elimination medicament for eyes, which comprises the following components by weight percent: 6% of golden cypress, 6% of Scutellaria laterifolia, 6% of coptis, 6% of selfheal, 6% of physalis peruviana, 6% of rhizoma polygoni paleacei, 6% of sophorae flavescentis, 14% of java brucea, 6% of raspberry, 6% of dandelion, 6% of amber, 3% of dried alum, 3% of borax, 2% of sal ammoniac and 18% of calamine. The invention has the efficacies of rapid toxicant removal and elimination, sterilization and antiphlogosis, can cure the eye diseases, has unique curative effect, and is suitable for the patients of glaucoma, cataract, floaters symptom, pterygium and the like.
US20080312087 2-Propenal and Related Enal Compounds for Controlling Plant Pests and Weeds in Soil A method for controlling pests and weeds on or around plants, especially crop plants is disclosed. The method includes admixing 2-propenal or other related enal compounds to form an aqueous solution, and applying the aqueous solution to plants, plant seeds, weeds, or soil around the around the area in which the plants grow.
US20110071181 Effervescent oral opiate dosage forms and methods of administering opiates Opiate containing dosage forms and methods using same are described. These dosage forms include substantially less opiates by weight than known oral formulations. These dosage forms are intended for oral administration across the oral mucosa.
EP1311708B1 Method for identifying substances useful for treating inflammation using the response element to the ikappabaplha ror receptor The invention concerns a method for identifying substances useful for treating inflammation, characterised in that it comprises the following steps: (a) contacting said substance with a nucleic acid construct containing the response element to the ROR receptor of the promoter of the I kappa B alpha gene in conditions suitable for allowing said substance to be fixed on the response element; (b) measuring the possible fixing of said substance on the response element or the transcriptional activity of the response element or of a promoter containing it; (c) optionally comparing the measurement of step (b) with a measurement carried out in conditions similar to those of steps (a) and (b) but with a nucleic acid construct non containing the mutated response element.
EP1676574A2 Methods for promoting survival of transplanted tissues and cells Methods for enhancing the survival of a cell, tissue, or organ transplanted into a recipient comprising contacting the cell, tissue, or organ graft with an agent that decreases the rate of coagulation on the transplanted cell, tissue or organ are disclosed. The agent is one that acts by reducing the amount or activity of tissue factor (TF) on the donor tissue, such as a p38 MAPK inhibitor, a JNK inhibitor, a p38 MAPK/JNK dual inhibitor and a TF antagonist. Cells, tissues and organs treated with those agents are also disclosed.
US20100120903 Anti-inflammatory agent An anti-inflammatory agent which includes an oil-soluble licorice extract, prepared by subjecting at least one of a leguminous plant of the genus Glycyrrhiza and a water extraction residue of a leguminous plant of the genus Glycyrrhiza to an extraction treatment with an organic solvent and which has at least one effect selected from an inhibitory effect on hyaluronidase activity, an inhibitory effect on hexosaminidase release (i.e., inhibitory effect on histamine release), an inhibitory effect on platelet aggregation, and an inhibitory effect on phospholipase A2 activity.
EP2454254A2 Benzimidazole analogues for the treatment or prevention of flavivirus infections Compounds represented by formula (I) or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B', X, Y, R1, R1 ', R2, R2', R3, R3', R5, R5', R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
US20120157426 Mutant-selective egfr inhibitors and uses thereof The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
CN102028685A Application of Gimeracil The invention discloses a new application of Gimeracil, which is characterized by an application of the Gimeracil in preparing antitumor drugs, wherein the drugs in unit dose form are prepared from the Gimeracil, and the unit dose is 1-500 mg. Pharmacological experiments indicate good antitumor activity of the Gimeracil.
CN101836966A Agomelatine-containing orally disintegrating tablet The invention provides an agomelatine-containing orally disintegrating tablet, which is characterized in that the inclusion technology is adopted to prepare the agomelatine-containing orally disintegrating tablet. The invention effectively covers up the tingling of agomelatine, improves the dissolution of the agomelatine, and is suitable for industrial production.
CA2306628C Cosmetic formulations for the prevention and therapy of hair loss The present invention provides new formulations useful in the prevention and therapy of hair loss and seborrhoea, which are based on essential oils obtainable through alcoholic distillation of the plants which contain the essential oils, combined with salicylic acid and with fatty acids having 10 to 14 carbon atoms.
WO2013041204A1 Novel isocyanate and isothiocyanate compounds for cancer treatment The invention relates to novel isocyanate and isothiocyanate compounds, pharmaceutical compositions comprising same, and the use thereof for the treatment of cancer in humans and animals. Compared with previously known isocyanate and isothiocyanate compounds, the novel isocyanate and isothiocyanate compounds are characterized by greater therapeutic breadth, i.e. fewer side effects and high antitumor activity.
US20100168105 Spirocyclopropyl Piperidine Derivatives Disclosed herein is at least one piperidine derivative, at least one pharmaceutical composition comprising at least one piperidine derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith
CN1752085A Aromatic hydrazide kind compound and its use in preparation of immune inhibitor An aroylhydrazine compound, its geometric isomer or its pharmacological salt or hydrate, its preparing process, and the composite medicine containing it for treating the organ transplant rejection and preventing and treating some autoimmunopathies including rheumatoid disease, psoriasis, multiple sclerosis, lupus erythematosus, etc are disclosed.
US20080033031 Antibiotic compounds, compositions and methods of treatment Antibiotic compounds and compositions and methods for the treatment of dermatological conditions including a sulfoxide or sulfone derivative of an antibiotic from the lincomycin family of antibiotics, or pharmaceutically acceptable salts thereof, optionally including a peroxide component.
EP1797042A1 Indozolone derivatives as 11b-hsd1 inhibitors Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R7 have the significances given in the description and claims can be used in the form of pharmaceutical compositions. The compounds of formula (I) are 11b-HSD1 inhibitors.
WO2014037927A1 Chlorate compositions and use of chlorate for treating radiation exposure The present application relates to the use of chlorate for treating subjects who have been exposed to radiation. More particularly, the application relates to the use of chlorate for treating subjects with acute radiation syndrome. The application also relates to compositions comprising chlorate and methods of using the compositions to treat subjects who have been exposed to radiation.
WO2012136121A1 Amino phenylpropanoid compound and use thereof for preparing immunosuppressant An amino phenylpropanoid compound, or a geometric isomer thereof, or a pharmaceutically acceptable salt or hydrate thereof as represented by Formula I, a preparation method therefor, and a pharmaceutical composition containing the compound. The compound is used to act as an immunosuppressant, applicable in preparing an organ transplant anti-rejection medicament and medicaments for treating and/or preventing certain autoimmune diseases such as rheumatoid, psoriasis, multiple sclerosis, and systemic lupus erythematosus. [Formula I]
WO2004080467A3 Method of treating and preventing hyperparathyroidism with vitamin d2 or d4 compounds This invention relates to a method for treating or preventing hyperthyroidism associated with chronic kidney disease by administering a sufficient amount of a vitamin D2 or vitamin D4 compound, the chronic kidney disease being stages 1-4.
CN103536570A Cimetidine composition lyophilized oral-disintegration tablets The invention provides cimetidine composition lyophilized oral-disintegration tablets, and relates to the technical field of medicine and medicine preparation. The tablets comprise the raw materials of, by weight: 200-800g of cimetidine, 150-600g of microcrystalline cellulose (100 mesh), 800-4000g of dextrin (100 mesh), 50-200g of chitosan nano-particles, proper amount of citric acid, and 1000-2000mL of injection water. The tablets has the advantages of high disintegration speed, high dissolution rate, good stability, accurate dose, uniform content, convenient application, easy carrying, easy-to-obtain raw materials, and low cost. A cimetidine composition lyophilized oral-disintegration tablet preparation method has the advantages of simple operation, easy control, labor saving, and time saving. The method is suitable for large-scale industrialized productions.
CN102988547A Preparation method of medicinal dragon bone powder for treating herpes zoster The invention relates to a preparation method of medicinal dragon bone powder for treating herpes zoster. The preparation method comprises the following steps: drying crude dragon bone, centipede, realgar and the like, and co-grinding the above raw materials into extremely fine powder, uniformly mixing, putting the obtained mixed powder into a bottle, and carrying out seal storage. The medicinal dragon bone powder is smeared on affect parts when the medicinal dragon bone powder is used. The medicinal dragon bone powder is convenient to use, has a substantial curative effect, and is a good method for treating the herpes zoster.
CN103222999A Honeysuckle extractant and preparation method and application thereof The invention discloses a honeysuckle extractant and skin medicine, and the honeysuckle extractant comprises the following components by weight: 20-50 parts of chlorogenic acid; 1-5 parts of oleanolic acid; 0.001-5 parts of ursolic acid. The invention also provides a preparation method of honeysuckle extractant, which comprises the following steps: extracting honeysuckle by alcohol-containing polar solvent using ultrasonic wave for obtaining honeysuckle extractant, wherein, the ultrasonic extraction temperature is in the range of 15-45 DEG C., purifying honeysuckle extractant using molecularly imprinted macromolecule for obtaining honeysuckle extractant.
US7202236 Salts of inhibitors of trypsin-like proteases such as thrombin, e.g., a sulfonate salt of Ph(3-Cl)(5-OCHF2) (R)CH(OH)C(O) (S)Aze-Pab(OMe), combined with a cellulose ether neutral gelling polymer for the treatment or prevention of thrombosis A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R1 represents C?1-2#191 alkyl substituted by one or more fluoro substituents; R2 represents hydrogen, hydroxy, methoxy or ethoxy; and n represents 0, 1 or 2; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable diluent or carrier, provided that the formulation may only contain iota-carrageenan and a neutral gelling polymer when the compound of formula (I) is in the form of a salt; such formulations being of use for the treatment of a cardiovascular disorder
CN102712640A Tricyclic heterocyclic compounds, compositions and methods of use thereof The invention provides novel compounds of formula (I) having the general formula, wherein R1, R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
US20050165011 6-[5-(6-methyl-pyridin-2-yl)-1H-[1,2,3]triazol-4-yl]-4H-benzo[1,4]oxazin-3-one, used as inhibitors of the transforming growth factor beta-signalling pathways, in particular, the phosphorylation of smad gene and proteins or activin-like kinase receptors; prophylaxis of kidney fibrosis This invention relates to benzoxazine and benzoxazinone substituted triazoles which are inhibitors of the transforming growth factor, (“TGF”)-β signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β, type I or activin-like kinase (“ALK”)-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.
WO2012116196A2 Substituted lactosyl compounds and use thereof for cellular imaging and therapy The invention provides methods for producing compounds comprising a substitution at the 1'-position of a lactosyl ring. Also provided are compounds having a radionuclide, such as 18F substituted at the 1'-position of a lactosyl ring. Compounds according to the invention may be used as therapeutics or imaging agents, such as PET imaging agents. Methods for therapeutic and diagnostic use of substituted lactosyl compounds are also provided.
US20080214625 Administering [3-cyclopropylmethoxy-4-difluoromethoxy-N-(3,5-dichloropyrid-4-yl)benzamide; hypertension, hyperlipidemia, hyperuricemia, gout and hypercoagulability The invention relates to the use of Roflumilast and/or Roflumilast N-Oxide for the treatment of diabetes mellitus and accompanying disorders thereof. The invention additionally relates to combinations of Roflumilast and/or Roflumilast N-Oxide with other active agents for the treatment of diabetes mellitus.
US20100222284 Composition for inhibiting the onset of arteriosclerosis and inhibition method [Object] To provide a composition for inhibiting the onset of arteriosclerosis by using a rare sugar D-psicose and a method of inhibiting the onset of arteriosclerosis. [Means for Resolution] The composition for inhibiting the onset of arteriosclerosis is characterized by comprising D-psicose as an active ingredient for an antiatherogenic action. The antiatherogenic action as described above includes an action of inhibiting or reducing the expression of a chemokine or a cytokine related to arteriosclerosis in vivo and an action of promoting the expression of a receptor involved in the improvement of arteriosclerosis without affecting the expression of an arteriosclerosis inducer. This composition is used in the form of a product selected from the group consisting of sweeteners, seasonings, food additives, food materials, foods and drinks, health foods and drinks, drugs, quasi drugs and feeds blended with D-psicose and/or its derivative and/or a mixture thereof as the active ingredient. The method of inhibiting the onset of arteriosclerosis is a method of using the above composition.
EP2004641A1 Hiv inhibiting 5-(hydroxymethylene and aminomethylene) substituted pyrimidines This invention concerns 5-(hydroxymethylene and aminomethylene)pyrimidine derivatives having HIV (Human Immunodeficiency Virus) replication inhibiting properties, to the preparation thereof and to pharmaceutical compositions comprising these compounds.
CN101940556B Preparation method of diammonium glycyrrhizinate freeze-dried powder injection The invention discloses a preparation method of diammonium glycyrrhizinate freeze-dried powder injection, comprising the following steps: (a) dissolving a diammonium glycyrrhizinate raw material in water for injection with preset volume, and controlling a pH value to 5.5-7.5; (b) adding activated carbon for injection for filtration, and decarbonizing; (c) finely filtering with a filter membrane of 0.22mum, and then ultra-filtering with ultrafiltration equipment with 5000-10000 in molecular weight cut-off; (d) sub-packaging the obtained filtrate; and (e) carrying out freeze drying, pressing and leaving the package. The diammonium glycyrrhizinate freeze-dried powder injection obtained by the method of the invention requires no an excipient and has beautiful frozen shape, good redissolution property and high product qualification rate.
EP1805159A1 Substituted carboxylic acids The present invention relates to compounds and pharmaceutically acceptable salts of formula I: which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention are also useful in pharmaceutical compositions and methods of treating the aforementioned conditions.
EP1173441B1 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations This invention describes the new 6-alkenyl- and 6-alkinyl- epothilone derivatives of general formula (I) in which R?1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7¿, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.
EP2224960A2 Method of treating cancer A method and composition for administering a therapeutic agent to a lesion comprising a contrast/carrier agent and ethanol.
US6875793 Once-a-day controlled release sulfonylurea formulation This invention is directed to a novel solid matrixed controlled release, oral dosage form where the dosage form contains a therapeutically effective amount of a sulfonylurea or a salt or derivative thereof in the matrix. Further, the use of an aqueous alkalizing medium affords substantially complete bioavailability of the drug from the matrix of the tablet. The core tablets may optionally be coated with a coating material in the range of 2% to 10% with an enteric material or with a water insoluble material like ethyl cellulose.
CN101985480A Mussel polysaccharide and preparation method and application thereof The invention provides a mussel polysaccharide. The polysaccharide content of the mussel polysaccharide is detected by an ultraviolet spectrophotometer and the polysaccharide is 55 to 90 percent based on glucose (C6H12O6). Monosaccharide components in the mussel polysaccharide, which are detected by high performance liquid chromatography, comprise the glucose, glucuronic acid, glucosamine and the like. The mussel polysaccharide is prepared by alcohol treatment, water extraction, pressure filtration, drying and other processes. Clinical verification results show that the mussel polysaccharide has definite curative effect of treating patients with syndrome of endogenous heat due to yin deficiency and the syndrome of endogenous heat due to yin deficiency accompanied with cancer pain, is convenient to take and safe, does not have any toxic or side effect and can be used for preparing medicaments for nourishing yin, clearing heat, diminishing swelling and relieving pain and the cancer pain.
EP2493572A1 Angiogenesis promoted by caged growth factors The present disclosure relates to controlling the release of growth factors for the promotion of angiogenesis. The growth factors or a polymer matrix are modified by photoactive compounds, such that the growth factors are not released into an active form until they are irradiated with light. The disclosure also relates to tissue engineering scaffolds comprising one or more polymers and at least two growth factors.
CN102145124B Health-care nursing liquid for hands and feet, preparation method and using method The invention discloses an external use health-care nursing liquid for hands and feet, a preparation method and relates to a health-care product. The preparation method comprises the following steps of: mixing divaricate saposhnikovia root, chaff flower root, obscured homalomenarhizome, clematis root, kadsura pepper stem, Chinese starjasmine stem, common clubmoss herb, common curculigo rhizome, rose-of-sharon root bark, belvedere fruit, gentian root, common bletilla pseudobulb, Japanese ampelopsis root, mentha leaves, flos caryophyllata, lotus stamen, rhizoma kaempferiae and borneol, adding water which is 20 to 30 times of the total weight of the mixture, decocting, adding table vinegar, and filtering to remove dregs of decoction; and adding 50-degree distilled spirits to prepare the external use health-care nursing liquid for the hands and feet. The external use health-care nursing liquid for the hands and feet can eliminate pruritus by sterilizing and disinfecting, remove squama and white scalesby sterilizing, dispel wind and remove dryness-heat, remove dead skin, sclerodermite and putrid skin and promote tissue regeneration; and by using the external use health-care nursing liquid, the conditions of the feet are changed obviously, exuviae falls off, the skin is reddish and bright and clean, and planta pedis has the comfortable soft and warm feeling. The external use health-care nursing liquid for the hands and feet also has the effects of warming main and collateral channels, promoting blood circulation and removing blood stasis, dispelling wind and relieving pain, improving microcirculation, enhancing the immunity of bodies, warming and tonifying kidney and controlling water metabolism by kidney, and water is dissolved in the skin, so the health-care nursing liquid has the nourishing effect on the skin.
US8383100 Method to treat and prevent skin diseases with Porifera-based therapeutic compositions treating and preventing skin diseases Methods to treat skin conditions and diseases by applying Porifera based compositions to the skin are described. Treatable skin conditions and diseases include acne vulgaris, rosacea, seborrheic dermatitis, atopic dermatitis, psoriasis, photo-aging, actinic keratosis and eczema, also known as atopic dermatitis. Therapeutic compositions are obtained from members of Porifera, for example sponges, specifically, fresh water sponges. An example of a fresh water sponge is Spongilla species. One specific therapeutic composition is obtained from Spongilla species and formulated with pharmaceutical excipients.
CN102846626A Inhalation preparation containing sodium mercaptoethane sulfonate and Fluticasone propionate The invention discloses an inhalation preparation containing sodium mercaptoethane sulfonate and Fluticasone propionate. Active ingredients (sodium mercaptoethane sulfonate and Fluticasone propionate) and one or more pharmaceutical adjuvants suitable for inhalation constitute the inventive preparation.
CN101422454A Omega-3 polyunsaturated fatty acid tanshinone IIA sub-microemulsion and preparation method thereof The invention discloses a stable Tanshinone IIA submicron emulsion and a preparation method thereof. The characteristic of Omega-3 polyunsaturated fatty acid for dissolving high-purity Tanshinone IIA is utilized and the pharmacological action of the Omega-3 polyunsaturated fatty acid is combined for preparing the stable Tanshinone IIA submicron emulsion. The stable Tanshinone IIA submicron emulsion of the Omega-3 polyunsaturated fatty acid obtained by the invention has better stability; animal test proves that the stable Tanshinone IIA submicron emulsion has no anaphylactic reaction, no hemolytic reaction and no agglutination reaction, and has no local thrill; and the stable Tanshinone IIA submicron emulsion not only can be prepared into an injection preparation, but also can be prepared into an oral dripping agent.
CN101766586A Ciclesonide capsule type inhalation aerosol powder and preparation method thereof The invention discloses ciclesonide capsule type inhalation aerosol powder and a preparation method thereof. The ciclesonide capsule type inhalation aerosol powder can improve the deposition rate of ciclesonide in the inhalation aerosol powder in lung, avoid the deposition of carrier micropowder in the lung, improve the stability of a composition and consists of an active component and micropowder of a carrier and is characterized in that the average particle diameter of the micropowder as the active component is 0.5-10mu m and the average particle diameter of the micropowder of the carrier is 20-45mu m.
CN102028678B Application of salvianolic acid A in preparing anti-tumor metastasis medicine The invention discloses an application of salvianolic acid A in preparing an anti-tumor metastasis medicine. The invention has the importance of discovering that the salvianolic acid A in salvia miltiorrhiza has notable inhibiting effect on tumor metastasis, has obvious influence on the tumor metastasis related gene and protein, can selectively inhibit proliferation of tumor cells, and has safetyand low toxicity to normal cells of the human body, so that the salvianolic acid A has application prospects in preparing the anti-tumor metastasis medicine.
EP1240168B1 Bicyclic inhibitors of glycogen synthase kinase 3 Bicyclic based compounds of the formula (I), compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and a treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
US20110033552 Apatite/collagen composite powder, formable-to-any-shape artificial bone paste, and their production methods An apatite/collagen composite powder absorbed and replaced by autogenous bone in the living body, a formable-to-any-shape artificial bone paste comprising an apatite/collagen composite powder and a binder, a method for producing an apatite/collagen composite powder by turning a suspension containing a fibrous apatite/collagen composite to liquid drops and rapidly cooling them, and a method for producing an apatite/collagen composite powder by granulating a blend comprising a fibrous apatite/collagen composite.
WO2009005470A1 Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors This invention relates to novel compounds having the structural formula I below: (Formula I), and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
EP1102758B1 Particle-forming compositions containing fused pyrrolocarbazoles A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that provides greatly improved bioavailability of orally administered fused pyrrolocarbazole compounds.
WO2008013280A1 Substituted spiroketal derivative and use thereof as drug for treating diabetes Disclosed is a compound represented by the formula (II) below, a pharmaceutically acceptable salt thereof, or a solvate thereof. Also disclosed are a pharmaceutical product, a pharmaceutical composition and the like, each containing the compound. [In the formula (II), R1 represents a chlorine atom, a fluorine atom, a methyl group or an ethynyl group; Ar represents a group represented by the following formula (a), formula (b), formula (c) or formula (d); R2 represents a C1-6 alkyl group which may be substituted with one or more halogen atoms, a C1-6 alkoxy group which may be substituted with one or more halogen atoms, a C1-3 alkylthio group, a halogen atom, a C1-3 alkylcarbonyl group or a C2-5 alkynyl group which may be substituted with -OR4; R3 represents a hydrogen atom or a C1-3 alkyl group; and R4 represents a hydrogen atom or a C1-3 alkyl group. In this connection, when R1 is a fluorine atom, a methyl group or a ethynyl group, Ar is a group represented by the formula (a), and when R1 is a methyl group, R2 is a methoxy group, anethoxy group, an isopropyl group, a propyl group, a trifluoromethyl group, a trifluoromethoxy group, a 2-fluoroethyl group or a 1-propynyl group.]
CA2322633C An iron-dextran compound for use as a component in a therapeutical composition for prophylaxis or treatment of iron-deficiency, a process for producing said iron-dextran compound and use of said compound for the preparation of a parenterally administrable therapeutical composition An iron-dextran compound for parenteral treatment of iron-deficiency anemia comprises hydrogenated dextran having a weight average molecular weight (Mw) between 700 and 1,400 Daltons, preferably approximately 1,000 Daltons, a number average molecular weight (Mn) of 400 to 1,400 Daltons and wherein 90 % by weight of the dextran has molecular weights less than 2,700 Daltons and the Mw of the 10 % by weight fraction of the dextran having the highest molecular weights is below 3,200 Daltons, said hydrogenated dextran having been subjected to purification by membrane processes having a cut-off value between 340 and 800 Daltons, in stable association with ferric oxyhydroxide. The compound is produced by using membrane processes to eliminate dextrans of higher molecular weights than approximately 2,700 Daltons and membrane processes to remove saccharides of molecular weights below approximately 340 Daltons from hydrogenated dextran before precipitating ferric hydroxide in the presence of said dextran followed by heat treatment and purification.
US20070275893 Compositions for enhanced epithelial permeation of peptide yy for treating obesity Pharmaceutical compositions comprising PYY(3-36), a cyclodextrin, and a compound selected from phosphatidylcholine or diglyceride, wherein the PYY(3-36) is present in an amount effective to alleviate one or more symptom(s) of obesity in a subject, and the cyclodextrin and the compound selected from phosphatidylcholine or diglyceride are present in an amount sufficient to enhance epithelial permeation.
US20130041001 Valsartan derivatives carrying nitrogen oxide donors for the treatment of vascular and metabolic diseases Nitrate esters and diazeniumdiolate derivatives of valsartanamide are described. They have valuable properties in the treatment of vascular and metabolic diseases.
US7538124 N-(p-(2-alpha-carboxybenzylamino)ethylamino)phenyl)p-(p-trifluoromethylphenyl)benzamide; hyperlipidemia; antiobesity and anti-type II diabetic agents; Microsomal triglyceride transfer protein inhibitors Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.
EP1017394B1 Cyclin dependent kinase inhibiting purine derivatives A range is disclosed of purine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDKs) and which thereby c an provide useful therapeutic compounds for use in treatment of tumours or other cell proliferation disorders. The compounds of this invention bind to CDK molecules in a manner that appears to be different to that of known CDK inhibitors such as olomoucine and roscovitine. In formula (I), in preferred embodiments: X is O, S or CHRx where Rx is H or C1-4 alkyl; D is H, halo or NZ1Z2 where Z1 and Z2 are each independently H or C1-4 alkyl or C1-4 hydroxyalkyl; A is selected from H, C1-4 alkyl, C1-4 alkoxy, hydroxy, CH2(CH2)nOH (n=1-4), and NRa1Ra2 where Ra1 and Ra2 are each independently H or C1-4 alkyl; B is selected from H, C1-4 alkyl, C1-4 alkoxy, CF3, an optionally substituted aryl (e.g. phenyl) or an optionally substituted aralkyl (e.g. benzyl), and an hydroxy group that provides a C=O tautomer; and Y is or includes an optionally substituted 4- to 8-membered carbocyclic or heterocyclic ring; or comprises an optionally substituted linear or branched hydrocarbon chain.
CN101879216A Compound natural essential oil with functions of refreshing brain and restoring consciousness The invention provides a natural essential oil with the functions of refreshing brain and restoring consciousness, which mainly consists of mint essential oil, glutaric acid mint ester, acetic acid mint ester and eucalyptus oil. The compound natural essential oil is characterized in that the natural essential oil can be matched with the other different plant essential oils to form into essential oils with different odor types, wherein the essential oils with different odor types comprise the following components based on parts by weight: 45-85 parts of mint oil, 2-8 parts of glutaric acid mint ester, 1-5 parts of acetic acid mint ester, 1-5 parts of eucalyptus oil, and the balance different plant essential oils. The compound natural essential oil has the advantage of being a product with the functions of refreshing brain and restoring consciousness, which is specially designed for the crowd such as drivers, students, public functionary, night workers and the like. The compound natural essential oil has unique prescription, and furthest improves the part which is good for refreshing brain and restoring consciousness, has less acrimony to the skin and the smell, and has pure and strong flavor. The compound natural essential oil smells good and has a remarkable effect for refreshing brain and restoring consciousness when in use. By being matched with various purely natural plant essential oils such as the rose, the jasmine, the lemon and the like, the compound natural essential oil is better for refreshing brain and restoring consciousness.
US20080070980 or esters; promoting an increased protein formation and/or prevention of loss of proteins in humans and animals due to an adverse health condition; increased protein formation in sports and workout activities; during aging β-Cryptoxanthin and esters thereof may find use for promoting an increased protein formation and/or prevention of loss of proteins in humans and animals.
US20100203060 Inhibitors for growth hormone and related hormones, and methods of use thereof The present invention encompasses novel inhibitors for growth hormone and related hormones, including prolactin, and placental lactogen, and other hormones. The invention specifically encompasses antibodies, antibody fragments, and modifications thereof, as well as polynucleotides, such antisense polynucleotides, interfering RNAs, and small interfering RNAs, and uses thereof, for inhibition of one or more of such hormones. In particular aspects, the invention encompasses methods of producing such inhibitors, compositions comprising one or more of these inhibitors, and methods of inhibiting a cell, e.g., inhibiting cell proliferation, cell survival, or cell motility, especially for a cancer cell, using one or more of the inhibitors. The invention also encompasses methods of diagnosis and monitoring, and methods of treatment, especially for cancer, using one or more of the disclosed compositions or inhibitors.
US20090312379 Dimeric Small Molecule Potentiators of Apoptosis Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
CN101723997A Puerarin glycosylation derivative, medicine compound, preparation method and application thereof The invention discloses a puerarin glycosylation derivative, a medicine compound thereof, a preparation method and application thereof, in particular to the puerarin glycosylation derivative of Formula (I) or a medical acceptable salt thereof, wherein R is a monose base (hexose or pentose) or an oligose base (connecting 2 to 5 hexose or pentose ). The medical acceptable salt is compounded salt of inorganic base or organic base. The puerarin glycosylation derivative or the medical acceptable salt thereof of the invention has better stability and water-solubility, promotes the bioavailability and enhances the healing effect.
WO2012007453A1 Crystalline compound of 1-[4-(2-azepan-1-ylethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol The present invention relates to a crystalline compound of 1-[4-(2-azepan-1 - ylethoxy)benzyl] -2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol (INN: bazedoxifene) of formula (1) with an acid selected from the group consisting of propionic acid or nicotinic acid or a hydrate thereof, where the molar ratio of the compound of formula (1) to the acid is 1:0.9 to 1:1.1, and to a process for its preparation.
CN103121965A Salts of indolone derivatives The invention relates to (E)-1, 3-dihydro-5, 6-dimethoxy-3-[(4-hydroxyphenyl) methylene]-2H-indol-2-ketone, fumarates of derivatives thereof or pharmaceutically acceptable solvates thereof and an application thereof to preparation of a medicament for treating cancer.
WO2011138565A1 Pharmaceutical combination containing lipoic acid, hydroxycitric acid and a somatostatin as active ingredients A pharmaceutical combination containing lipoic acid, hydroxycitric acid and a somatostatin analogue as active ingredients. The subject matter of the present invention is a novel pharmaceutical combination and the use thereof as an antitumour composition. According to the invention, this combination comprises, as active ingredients, lipoic acid or a pharmaceutically acceptable salt thereof; hydroxycitric acid or a pharmaceutically acceptable salt thereof; and somatostatin or an analogue thereof or a pharmaceutically acceptable salt of said somatostatin or of said analogue thereof.
EP1889635A1 Haemodialysis concentrates The present invention relates to haemodialysis concentrates used to make ready-for-use haemodialysis solutions applicable in patients with both acute and chronic renal failure, diabetes and intoxication. The obtained haemodialysis concentrates contain according to the invention electrolytes, a buffer, an osmotic agent, and an antioxidant selected from the group including glutathione, N-acetyl-L-cysteine, and its pharmaceutically acceptable salts or α-lipoic acid and is in dry or liquid form. They are used to prepare a haemodialysis solution to reduce undesirable complications of renal failure including cardiovascular diseases, renal anaemia, renal osteodystrophy, microinflammatory processes, malnutrition, polyneuropathy, and/or encephalopathy. The haemodialysis concentrates and the haemodialysis solutions prepared therefrom according to the present invention are stable and undergo no physicochemical changes and interactions.
US20080033032 Novel Polymorphs Of The Potassium Salt Of Atorvastatin Novel polymorphs Forms I, II and III of the potassium salt of Atorvastatin, (βR,δR)-2-(p-fluorophenyl)-β, δ-dihydroxy-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)pyrrole-1-heptanoic acid, are obtained directly by precipitation of the potassium salt of Atorvastatin with ethanol (polymorph I), with 1-propanol (polymorph II) and by recrystallisation of polymorph I from 2-propanol (polymorph III).
CN102114001A Orally administered solid preparation containing tolvaptan The invention discloses an orally administered solid preparation containing tolvaptan and a preparation method thereof. After micronization, the tolvaptan particles are prepared into the oral solid preparation with pharmaceutically acceptable excipients. More than 90% of the micronized tolvaptan particles has a diameter less than 75 micrometers, and the tolvaptan particles are obtained by wet granulation. The orally administered solid preparation is cinically used for the treatment of hyponatremia.
US20090012055 Piperidine derivatives such as 4-{4-[3-(2-Methoxybenzyloxy)propoxy]phenyl}-3-[3-methoxy-5-(3-methoxypropoxy)benzyloxy]piperidine, suitable as renin inhibitors, used for the treatment of hypertension, heart failure, glaucoma, cardiac infarction, kidney failure or restenosis; improved pharmacokinetics Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.
CN103275157A Rupestonic acid amide derivative containing heterocyclic ring and sugar, preparation method and purposes thereof The invention relates to a rupestonic acid amide derivative containing a heterocyclic ring and sugar, a preparation method and purposes thereof. The amide derivative containing a triazole heterocyclic ring and sugar is synthesized through the steps: at first, rupestonic acid and aminopropyne are in reaction to obtain a rupestonic acid derivative containing terminal alkyne, then, under the catalysis of copper sulfate and sodium L-ascorbate, rupestonic acid amide derivative containing a heterocyclic ring and peracetylated glycosyl is obtained, and further, acetyl is removed from methanol/sodium methoxide to obtain the target compound. The preparation method is mild in reaction condition, and the experimental procedure is simple. The derivative has anti-influenza virus activity, and can serve as anti-influenza virus drug used for treating influenza.
CN102451270A Preparation method of drug for treating eczema The invention relates to a preparation method of a drug for treating eczema. The preparation method comprises the following steps of calcining alum, stir-frying fructus evodiae with vinegar, mixing the calcined alum, the stir-fried fructus evodiae, bark of Chinese corktree, radix sophorae flavescentis, honeysuckle flower and borneol, and grinding the mixture into fine powder. A use method of the drug for treating eczema is characterized in that when exudate exists on an affected part, the drug for treating eczema is processed into dry powder and is sprinkled on the affected part; and when the exudate does not exist on the affected part, the drug for treating eczema is mixed with sesame oil and is applied on the affected part. The drug for treating eczema has the functions of astringing to arrest bleeding, resolving dampness and relieving itching, clearing heat and removing toxins, removing wind and killing parasites, and eliminating putridity and engendering flesh. The drug for treating eczema has very ideal effects of treating various eczema diseases.
US20100166727 S-Adenosylmethionine And Methylthioadensosine In Chemoprevention And Treatment Of Colon Polyps And Cancer The present invention relates to S-adenosylmethionine (SAMe), methylthioadenosine (MTA) for the treatment of disease. More specifically, the invention relates to SAMe and MTA methods and compositions for the chemoprevention and treatment of colon polyps and cancer.
EP1290952B1 Compositions for taking dietary fibers Compositions for taking dietary fibers which contain from 1 to 50% by weight, on the basis of the whole composition, of dietary fibers comprising water-soluble and hardly fermentable dietary fiber and water-soluble and fermentable dietary fiber, characterized in that the content of the water-soluble and fermentable dietary fiber ranges from 0.1 to 3 parts by weight per part by weight of the water-soluble and hardly fermentable dietary fiber. These compositions remarkably ameliorate not only bowel movement frequency but also full consciousness, feeling of unsatisfied defecation, etc. Thus these compositions are useful as foods for ameliorating bowel movement.
US7074933 quinolin-2-ones and chromen-2-ones compounds that have been derivatized at the 6-position with a urea or thiourea derivative; used as androgen antagonists; kits The invention is directed to a new class of quinolin-zene and z-exc chromen compounds that have been derivatized at the 6-position with a urea or this urea moet, and to then use as androgen antagonists.
WO2009090177A1 Bifeprunox derivatives The present invention relates to bifeprunox derivatives of the formula (I) wherein R1 is one substituent selected from 3-OH, 4-OH, 3-OSO3H and 4-OSO3H; R2 is H; or an N-oxide or a pharmaceutically acceptable salt, a solvate or hydrate thereof, which are potent ligands for the dopamine D2 receptor, exhibiting strong partial dopamine D2 agonistic effects with a percentage agonism significantly higher than bifeprunox. The compounds of the invention may be used in the treatment, alleviation or prevention of dopamine D2 receptor mediated diseases and conditions requiring dopamine D2 agonistic effects.
CN103736098A Intranasal medicinal composition containing bilastine and mometasone furoate The invention provides an intranasal medicinal composition. The intranasal medicinal composition contains bilastine, mometasone furoate, and thaumatin serving as a bitterness and irritation alleviator.
WO2012112699A3 Method and apparatus for the delivery of photo-chemical (cross-linking) treatment to corneal tissue Systems and methods for delivering and infusing formulations containing riboflavin or its analogues, or other ophthalmic formulations, into corneal tissue are disclosed. Systems and methods are further disclosed to cross-link the corneal tissue through exposure to UVA irradiation. The systems and methods for formulation delivery employ micro-needle array delivery devices.
WO2009128057A3 Growth factor modulators for the treatment of anxiety, depression and cognitive disorders The invention provides a selective Sigma 1 or Dopamine D3 receptor agonist or a 5HT2c receptor ligand for use in the treatment of symptoms of anxiety and/or depression associated with an affective disorder and/or symptoms associated with cognitive impairment disorder. Particularly useful are diphenhydramine derivatives of Formula (I) and particularly (2-[(4-butylsulfanylphenyl)-phenyl-methyl] sulfanyl-N,N-dimethyl- ethanamin) (Captodiamine).
CA2396130C Preparation of irrigating solution for ocular surgery A one-pack irrigating solution preparation for ocular surgery of cataract, intraocular lens implantation, glaucoma, vitrectomy or penetrating keratoplasty, which is excellent in the protection of ocular tissues and corneal endothelial cells during and after the surgery and has a high in a living body safety. This preparation comprises an aqueous solution containing at least one compound selected from the group consisting of D-3-hydroxybutyric acid and its salts, bicarbonates, and calcium glycerophosphate and is stable under severe temperature conditions.
CA2358498C The preparation and use of radium-223 to target calcified tissues for pain palliation, bone cancer therapy, and bone surface conditioning Processes for the preparation, prepared solution, and the use of radium-223 for the treatment of calcified tumors, bone tumors. treatment of bones, bone surfaces and soft tissues are described.
US20080299170 Medical Devices and Coatings Therefor A coating for a medical device, the device generally being of the type which is to be used internally in a subject, includes a transglutaminase (TGase) inhibitor. The Tgase inhibitor effectively prevents the activity of any Tgase involved in clot formation or clot stability. Preferably, the transglutaminase inhibitor is a factor XIIIa inhibitor. The coating may be prepared by suitable processes such as esterification. The coating may be immobilized on a suitable medical device in a number of ways and is preferably included in a TGase inhibitor containing polymer. The coating may also include a suitable antimicrobial agent.
US20110033528 Stabilized picoplatin oral dosage form The invention provides an oral dosage form for the anti-cancer drug picoplatin comprising a core and a coating, the dosage form being free of redox-active metal salts. The core of the tablet is a substantially dry powder comprising about 10 to 60 wt % picoplatin wherein the picoplatin is a particulate of less than about 10 microns average particle diameter, about 40-80 wt % of a filler comprising a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate, and an effective amount of up to about 5 wt % of a lubricant. The dosage form can further include a dispersant.
US20110159056 Methods and materials for stimulating proliferation of stem cells Disclosed herein are methods and materials for influencing proliferation of stem cells. Specifically exemplified herein are compositions comprising cerium oxide nanoparticles which can be used to stimulate proliferation of stem cells under common culture conditions, or which can be utilized to improve therapeutic outcomes.
CN103012407A N-[4-(1H-pyrazolo[3,4-b]pyrazine-6-yl)-phenyl]-sulfonamides and application of N-[4-(1H-pyrazolo[3,4-b]pyrazine-6-yl)-phenyl]-sulfonamides as medicines The invention relates to N-[4-(1H-pyrazolo[3,4-b] pyrazine-6-yl)-phenyl]-sulfonamides of a formula I. In the formula I, Ar, R1, R2 and n have meanings as shown in the claims. The compounds of the formula I are compounds which are valuable, have pharmacological activity and can adjust the activity of protein kinase, particularly the activity of serum and glucocorticoid induced kinase (SGK), and more particularly the activity of serum and glucocorticoid induced kinase isoform (SGK-1, SGK1). The compounds are suitable for treating diseases with inappropriate activity of the SGK, such as degenerative joint diseases or inflammatory process such as osteoarthritis or rheumatism. The invention also relates to a method for preparing the compounds of the formula I, an application of the compounds serving as the medicines and medicine compositions containing the compounds.
EP2260845A2 Use of polyphenols for the treatment of alopecia The use of taurine and/or hypotaurine and their salts in oral compositions for the prevention and treatment of aging of the pilosebaceous unit and/or alopecia. - ACTIVITY : Endocrine-Gen. - MECHANISM OF ACTION : Hair follicle alteration regulator; proline incorporation is reduced whilst leucine incorporation is unaffected. Two groups of 36 women aged 18 - 40 years having fine, limp and seborrheic hair were treated either with a composition as described or a placebo based on maltodextrin. The active formulation contained, per unit dose, taurine (159 mg), green tea extract (30 % catechins; 375 mg), grapeseed extract (40 % procyanidin oligomers, 20% catechins; 150 mg), zinc (as zinc sulfate; 15 mg). The number of hairs removed by three sweeps of the comb were counted after 0, 3, and 6 months, and the results are shown in the figure. After six months the number of hairs removed from the treated subjects averaged 40.5, whilst the number from untreated subjects was 56.7.
EP1695974A1 1,8-Naphthyridines as CRF antagonists The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl, each of which may be substituted by I to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -C(O)R5, nitro, -NR6R7, cyano, and a group R8; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR6R7 or cyano; R2 and R3 corresponds to; R4 is hydrogen, C1-C6 alkyl, halogen or halo C1-C6 alkyl; R5 is a C1-C4 alkyl, -OR6 or -NR6R7; R6 is hydrogen or C1-C6 alkyl; R7 is hydrogen or C1-C6 alkyl; R8 is a 5-6 membered heterocycle, which may be saturated or may contain one to three double bonds, and which may be substituted by 1 or more R11 groups; R11 is C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, or C(O)NR6R7; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
US7378111 Regulation of GSK-3α activity for the treatment or prevention of Alzheimer's disease Provided is a novel use of therapeutic concentrations of an inhibitor of glycogen synthase kinase-3 (GSK-3), including lithium or any other GSK-3 inhibitor, to block, reduce or inhibit processing of amyloid precursor proteins to beta-amyloid (Aβ) peptides, which are now believed to be the principal cause of Alzheimer's disease, thereby providing methods useful for the prevention, inhibition or reversal of the disease. Also provided are methods of using agents that specifically target the α isoform of GSK-3, which is responsible for APP processing, making such selective GSK-3α-specific inhibitors especially useful in the treatment, prevention, and possible reversal of Alzheimer's disease. Further provided are kits and screening methods associated with the present methods.
WO2007007105A1 Use of 3,1ib-cis-dihydrotetrabenazine for the treatment of symptons of huntington' s disease The invention provides 3,1 lb-cis-dihydrotetrabenazine for use in halting or slowing the progress of one or more symptoms of Huntington's disease in a patient, and more particularly a symptom selected from involuntary movements such as involuntary chorea, tremors and twitches, and degeneration in gait.
US20130028854 Osmoprotective Complexes for Prevention of Mitochondrial Free Radical Damage Related Skin Aging The present invention discloses a method to inhibit a free radical, including a mitochondrial free radical, comprising administering to a subject in need thereof an effective amount of a composition comprising a compound of formula (I: a, b), an isomer, or a salt thereof:
US20110059159 Nanoscale bound bilayers, methods of use and production Methods for rapidly obtaining a nanoscale apolipoprotein bound phospholipid bilayer (NABB) associated with at least one membrane protein are provided. Also disclosed are methods for rapidly obtaining a NABB not associated with membrane proteins. Immunogenic compositions comprising NABBs with native conformational epitopes are also provided along with their methods of use.
WO2008066185A1 Method for prevention of discoloration with time of donepezil-containing skin adhesive preparation [PROBLEMS] To prevent the discoloration with time of a donepezil-containing skin adhesive preparation. [MEANS FOR SOLVING PROBLEMS] An adhesive layer comprising an adhesive agent and donepezil is added with at least one stabilizer selected from the group consisting of ascorbic acid or a metal salt or ester thereof, isoascorbic acid or a metal salt thereof, ethylenediaminetetraacetic acid or a metal salt thereof, 2-mercaptobenzimidazole, 3(2)-t-butyl-4-hydroxyanisole, 2,6-di-t-butyl-4-methylphenol, pentaerythritol tetrakis[3-(3',5'-di-t-butyl-4'-hydroxyphenyl)propionate], (±)-α-tocopherol, (±)-α-tocopherol acetate, rutin, hypophosphorous acid, a metabisulfite metal salt and a hydroxymethanesulfinate metal salt.
CA2214670C 2-cyano-3, 5-dihydroxyhex-2-enecarboxamide derivatives 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or disorders whose course involves increased connective tissue or cartilage degradation.
CN103721054A Method for preparing medicine for treating urticaria The invention discloses a method for preparing a medicine for treating urticaria. The medicine is mixed from the following components in parts by weight: 15-25 parts of fleece-flower root, 12-15 parts of medlar, 2-4 parts of ginseng, 10-12 parts of wreath goldenrod, 17-26 parts of fructus xanthii, 2-6 parts of broom cypress fruit, 10-15 parts of Chinese date, 20-25 parts of glossy privet fruit, 13-15 parts of schisandra chinensis, 3-6 parts of alum, 15-18 parts of poria, 18-26 parts of phaseolus calcaratus, 5-9 parts of polygonatum kingianum, and 10-15 parts of wild chrysanthemum. The medicine prepared by the preparation method has the effects of quickly eliminating urticaria wheal, does not have side effect to the body, and avoids relapse.
CN102503945A Compound capable of inhibiting epidermal growth factor receptor and application thereof The invention relates to a compound capable of inhibiting an epidermal growth factor receptor and an application thereof. The invention also relates to a medicament composition which comprises the compound capable of inhibiting the epidermal growth factor receptor or pharmaceutically acceptable salts and at least one pharmaceutically acceptable carrier. According to the invention, the administration route of the medicament composition comprises oral administration, nasal cavity inhalation, percutaneous absorption, lung administration and non-intestinal injection administration. The invention further relates to an application of the compound in the aspect of preventing and treating cancers related to EGFR (epidermal growth factor receptor) and related diseases thereof and an application of the medicament composition in the aspect of preventing and treating cancers related to EGFR and related diseases thereof.
DE102006030037A1 Oral product, useful for preventing and treating seborrheic dermatitis, comprises cobalamin and/or betaines Oral product (I) for preventing and treating seborrheic dermatitis, comprises cobalamin and/or betaines. - ACTIVITY : Dermatological. - MECHANISM OF ACTION : None given.
WO2013152838A1 Preparation for topical application to mucosa containing polyhexanide as active ingredient The present invention relates to an in particular pharmaceutical preparation for topical application in the non-frozen state to mucosa, primarily in the mouth, nose and/or throat cavity in humans, which has polyhexanide (polyhexamethylenebiguanide) or a derivative thereof, as (anti-infective) main active ingredient. The composition can comprise further additives and be present in solid or liquid form. Polyhexanide here preferably has an average molar mass of from 1800 to 5000 g/mol, in particular 2000 to 3700 g/mol and very particularly preferably from 2300 to 3100 g/mol. The preparations are suitable for irritations of the mucosa caused by potentially pathogenic microorganisms, but not by chlamydia, or else for inflammations as a result of such an infection.
WO2012149546A2 Small molecule trail gene induction by normal and tumor cells as an anticancer therapy Methods and compositions relating to TIC10 are described according to aspects of the present invention. The compositions and methods have utility in treating disease, particularly cancer in a subject in need thereof, including a human subject as well as subjects of other species. The compositions have utility in treating brain cancer in a subject in need thereof.
CN1931234A Medicine composition of red sage and puerarin The present invention belongs to the field of medicine technology, and is especially one kind of medicine composition for treating cardiac and cerebral vascular diseases and its preparations and preparation process. The medicine composition is prepared with red sage in 1500-15000 weight portions and puerarin in 100-1000 weight portions, and may be prepared into different pharmaceutically acceptable forms, preferably injection and orally taken preparation. The medicine composition may be also prepared with red sage extract and puerarin. The medicine composition has greatly raised synergistic effect and high stability.
US20110275581 Nuclear export inhibitors of topoisomerase ii alpha A method of treating cancer in a subject comprising the step of administering to the subject in need thereof an effective amount of a combination of a compound that binds a nuclear export signal (NES inhibitor) on topoisomerase IIα and a topoisomerase inhibitor. Twenty small molecule inhibitors (SMI) that bind to the two nuclear export sequences (NES) topo IIα have been identified from the NCI database using computer-generated molecular modeling. These SMI will improve the effectiveness of topo II directed therapeutics, particularly in the treatment of diseases such as multiple myeloma (MM). In vitro apoptosis assays indicate that these drugs may be effective as single agents or in combination with currently used cancer drugs that target topo II.
WO2009061934A1 Use of prodrugs of gaba b agonists for treating neuropathic and musculoskeletal pain Methods of treating neuropathic pain, musculoskeletal pain, and back spasm associated with musculoskeletal pain in a patient comprising orally administering a therapeutically effective dose of a prodrug of a GABAB agonist having a high oral bioavailability of the corresponding GABAB agonist are disclosed.
US20060276409 N-Hydroxy-N-(1-(2-carbamoylalkylaminocarbonyl)ethyl)formamides: [(Formyl-hydroxy-amino)-methyl]-3-cyclopentyl-propionic acid (1-dimethyl-carbamoyl-2,2-dimethyl-propyl)-amide; bacterial polypeptide deformylase inhibitors Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n-(ALK)m- wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, and m and n are independently 0 or 1; and A represents a group as defined in the specification.
CA2808251A1 Neuroprotective and neuro-restorative iron chelators and monoamine oxidase inhibitors and uses thereof 8-Hydroxy-quinoline derivatives and 8-ethers, 8-esters, 8-carbonates, 8-acyloxymethyl, 8- phosphates, (phosphoryloxy)methyl, and 8-carbamates derivatives thereof are described that exhibit iron chelation, neuroprotective, neurorestorative, apoptotic and/or selective MAO-AB inhibitory activities.
CN102058832A Medicine composition preparation and preparation method thereof The invention discloses a medicine composition preparation and a preparation method thereof. The medicine composition preparation comprises the following 15 material medicines: calculus bovis artifactus, pulvis fellis suis, baikal skullcap root, tuber of aromatic turmeric, cape jasmine fruit, borneol, goldthread, pearl, ocher, realgar, cinnabar, menthol crystal, gypsum, buffalo horn concentrated powder and mother-of-pearl. The preparation method of the medicine composition comprises the following steps of: firstly grouping the material medicines and respectively preparing into intermediates and medicine powder; mixing and processing with a conventional process; and finally adding conventional auxiliary materials and preparing into a preparation form which is acceptable pharmaceutically. Pharmacodynamic experiments prove that the medicine composition prepared with the method disclosed in the invention has the effects of clearing heat, resisting inflammation and thrombopoiesis and reducing blood pressure.
US20080070910 aromatic or heterocyclic/heterobicyclic carbamate compounds as protease inhibitors , useful for inhibiting the development of drug resistance of HIV in HIV infected animals; improved pharmacokinetics; protease inhibitors The present invention provides compounds of Formula (I): wherein A, X, Q, R2-R6, m, and W have the values described herein, as well as compositions comprising such compounds. The compounds are protease inhibitors and are useful for inhibiting the development of drug resistance in animals.
CN101156859A Hydrochloric acid chlorine imipramine sublingual piece and method for making same The invention discloses a chlorimipramine hydrochloride sublingual tablet which is characterized in that the chlorimipramine hydrochloride sublingual tablet consists of 12 to 14 percent of chlorimipramine hydrochloride and 86 to 88 percent of auxiliary material, wherein, the auxiliary material contains diluent, disintegrant, binding agent, lubricant, correctives, and colorant. The drug of the sublingual tablet is rapidly absorbed, and the damage of gastrointestinal tract digestive enzyme and liver first pass metabolism to the drug is avoided, thereby the bioavailability of the drug is improved.
CN101891728A Scutellarein derivative as well as preparation method and application thereof The invention relates to the research field of medicinal chemistry, in particular to a novel scutellarein-6-site derivative (I), as well as a preparation method and an application thereof to medicines for preventing and treating thrombus. Pharmacological test results show that compared with scutellarin and scutellarein, the compound has better function of inhibiting platelet aggregation. The scutellarein-6-site derivative (I) provided by the invention can be used for treating a series of diseases caused by the thrombus, such as myocardial infarction, ischemia injury and so on.
CA2343732C Substituted .gamma.-phenyl-.delta.-lactones and analogs thereof and uses related thereto .gamma.-Phenyl-substituted .DELTA.-lactones and analogs thereof, including lactams, are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.
US7202250 2-substituted, especially 2-amino-substituted, e.g., [N-(1-ethyl)propyl]-5-(2,4-dimethoxyphenyl)-3,6-dimethylpyrazine-2-amine; bind with high affinity and high selectivity to CRF1 receptors and are used to treat central nervous system disorders Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
CN102010348A Salicylamide ester type derivative and preparation method and application thereof The invention discloses a salicylamide ester type derivative and a preparation method thereof. The salicylamide ester type derivative has a general formula 1. The salicylamide ester type derivative can be disassociated into a salicylamide type compound with anti-tumor activity and a short-chain fatty acid type compound such as valproic acid, butyric acid and the like with effect of suppressing histone deacetylase activity; thus, the salicylamide ester type derivative disclosed by the invention can be used as an antineoplastic medicament with a double action mechanism.
US20090076114 Cis-1,2-substituted stilbene derivatives and their use in preparation of drugs for treatment and/or prevention of diabetes The present invention relates to cis-1,2-substituted stilbene derivatives, or their pharmaceutically acceptable salts, glucosides or solvates, a pharmaceutical composition comprising the compound, and use of said compound for preparation of a drug for treatment and/or prevention of diabetes or improvement of diabetic complications.
CN1895261A Use of pokeroot saponin A in preparation medicine for treating rheumatoid arthritis An application of the esculentoside A in preparing the medicine or food for treating rheumatoid arthritis is disclosed. Its chemical structure is also disclosed.
WO2012140300A1 Compounds and compositions for treating multiple myeloma The invention relates to compounds that are inhibitors of the enzyme carnitine palmitoyltransferase I (CPT I), to compounds that are inhibitors of gastric and/or pancreatic lipase, to the therapeutic uses of same, and to compositions and low-density lipoproteins (LDLs) comprising at least one compound that is an inhibitor of the enzyme carnitine palmitoyltransferase I (CPT I), at least one gastric lipase inhibitor or at least one inhibitor of the proteasome 26S. The invention also relates to the use of said compositions and LDLs in the treatment of a pathology that presents uncontrolled proliferation of plasma cells, and more specifically, in the treatment of multiple myeloma.
WO2012043780A1 Orally ingestible skin activator and process for production thereof Provided is an orally ingestible skin activator characterized by containing an acidic phospholipid at a content of 40 mass% or more. The acidic phospholipid is preferably a phosphatidic acid and/or lysophosphatidic acid.
CA2822725A1 Modulators and methods for the treatment of rosacea An in vitro method of screening of candidate compounds for the preventive or curative treatment of rosacea includes determination of the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea; such method also includes in vitro diagnosis or prognosis of this pathology.
WO2013126656A1 Pyridopyrimidinone inhibitors of kinases The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
US7618955 Association of an antithrombotic and aspirin The present invention relates to a new combination of an antithrombotic and aspirin and to pharmaceutical compositions comprising them.
CN101327237A Composition containing plant effective component and preparation method and use thereof The invention discloses a plant active component composite containing ginseng polysaccharide, total saponins of panax ginseng, and hydrolysate of ginsenoside. The invention also discloses a preparation method thereof and an application thereof for regulating the immunity of the organism and resisting tumor.
EP1778615A2 Oligomeric ketone compounds A novel keto8enic compound is provided having general: Formula R(OCH(CH3)CH2C(O))n-O-A wherein n is an integer of 3 to 10, A is the residue of a 3-keto alkan-1-o1 and R is selected from the group consisting of H, C1-C6 alkyl and acetoaeetyl- Prefered compounds are those wherein A is a residue is of 4-hydroxy-2 butanone. A particularly preferred compound is a 4-hydroxy-2-butanone ester of an R-3-hydroxybutyrate oligomer having general: Formula H(OCH(CH3)CH2C(O))n-O-CH2-CH2-(CO)-CH3 Nutraceutical and pharmaceutical compositions are provided for use in treating one or more of acute trauma, hemorrhagic shock, neurodegeneration, diabetes, and epilepsy, stroke, head trauma, myocardial infarction, congestive heart failure, pulmonary failure, kidney failure, obesity depression, pain and impaired cognition.
WO2013134219A1 Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof Imidazo[1,2-b]pyridazine-based compounds of the formula (I): are disclosed, wherein R1, R2 and R3 are defined herein. Compositions comprising the compounds and methods of their use to treat, manage and/or prevent diseases and disorders mediated by mediated by adaptor associated kinase 1 activity are also disclosed.
CN102871952A Flurbiprofen acetaminophen ester solid dispersion and preparation method thereof The invention relates to flurbiprofen acetaminophen ester solid dispersion and a preparation method thereof. Anti-inflammatory and analgesic prodrugs mainly comprise brand new compounds of flurbiprofen acetaminophen ester, and the flurbiprofen acetaminophen ester solid dispersion is prepared by adding hydrophilic carrier materials and by respectively adopting a solvent method, a solvent-melting method and a melting method and can be further prepared into oral tablets or capsules by being mixed with proper adjuvants. By the flurbiprofen acetaminophen ester solid dispersion and the preparation method thereof, solubility and dissolving-out speed of drugs can be obviously increased, the solubility of the drugs in water is increased by 10-100 times as compared with that of crude drugs, cumulative dissolving-out percentage of the drugs in dissolving-out media in 45 minutes is substantially increased accordingly, and finally oral absorbability of the drugs is improved.
US20080187581 Solid dosage form; active materials and solid on substrate A solid pharmaceutical dosage form comprises a substrate containing an active agent and a solid composition deposited onto areas of a surface of the substrate and containing an active agent.
US7629014 Defatted canola flake, protein, and phytate; isoelectric precipitation and/or ultrafiltration Crushed and de-fatted oilseed is extracted with water at neutral, mildly basic or mildly acidic pH; and is filtered. The filter media allows passage of small fragments of solid cell meat into the filtrate. The filtrate is treated with a base to increase pH to over pH 9, and solids are separated out. Protein is separated from other constituents of the liquid and concentrated, for example by heat-induced or isoelectric precipitation and/or ultrafiltration. The remaining liquid is rich in sugars. The process results in one or more protein products suited for human or animal food ingredients or for production of cosmetics, a sugar rich product suitable for fermentation or use as a feed ingredient, and a fiber-protein animal feed ingredient.
US20100016283 Compounds and uses thereof - 150 Formula (I) below: and their pharmaceutically acceptable salts or tautomers, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence and neurodegenerative disorders.
CN1827158A Compound forming agent with zedoary turmeric oil and method for preparing the same Disclosed is a compound forming agent with zedoary turmeric oil and method for preparation, which consists of mixing oil of aromatic turmeric, Span-80, glycerin, Tween-80 and sodium dodecylsulfate, stirring homogeneously, mixing Xiaoyikangcuo with right amount of ethanol and dissolving, mixing the two obtained solutions, stirring homogeneously, charging distilled water and mixing homogeneously, making foams through a hand net type foam emulsion generation device.
CA2427221C Process and intermediates for preparing anti-cancer compounds Disclosed are methods for preparing compounds of the formula 9
EP1128830B1 Reversing advanced glycosylation cross-links using heterocyclic-substituted thiazolium salts The present invention relates to compositions and methods for reversing advanced glycosylation end product-mediated cross-linking and protein aging. Accordingly, compositions are described which comprise thiazolium compounds substituted with heterocyclic groups which are capable of reversing the formation of advanced glycosylation end product cross-links. Both industrial and therapeutic applications for the invention are disclosed, as food spoilage and animal protein aging can be treated. Such compounds have particular application in the treatment of protein aging such as is responsible for the complications of aging and diabetes.
US8722087 Titration dosing regimen for controlled release tramadol A titration dosing regimen for the administration of controlled release tramadol analgesic to patients. The titration dosing regimen provides a significant reduction in the occurrence of adverse effects from the introduction of controlled released tramadol dosing, thus increasing patient compliance and medication tolerability.
US20100113548 Antagonists of bitter taste receptors and uses thereof The present invention relates to antagonists of the human bitter-taste receptors hTAS2R38. The invention also relates to methods for identifying further molecules that suppress hTAS2R38 mediated bitter taste transduction or bitter taste response and uses thereof.
CN101205237A Extraction of high-purity lecithin from animal livers The invention relates to a separation and purification process for animal liver lecithin (phosphatidylcholine), which is characterized in that a reasonable process (column chromatography, etc.) is adopted to purify the prepared high-precision lecithin with the livers of animals as raw materials and the single ethanol as eluent and the content of phosphatidylcholine can reach over 85 per cent. The invnetion has a simple process, delivers high precision and high yield, requires a low cost, and has an environmentally-friendly production process; the invention is also characterized by high product quality and significantly high practical and popularization values. For the time being, the lecithin is widely applied in the fields of medical care, agriculture, industry, etc., neverthless, the lecithin (phosphatidylcholine) contained in the livers of animals has performance indexes superior to those of the soybeans and the egg yolk lecithin and can be widely used in the fields of foods, health products, cosmetics, raw materials of anticancer drugs, etc., in particular, the lecithin (phosphatidylcholine) contained in the livers of animals has very favorable protective effects on the liver injuries and eminent antihepatocarcinamo effect, etc.
US20120141611 Methods and compositions using ergothioneine to treat a variety of health related factors In one embodiment, a composition containing ergothioneine and/or synthesized l-ergothioneine and one or more compounds selected from the group consisting of vitamin B-12, glucosamine sulfate, calcium ascorbate, turmeric extract, black pepper extract, hyaluronic acid, collagen, glycosaminoglycans, cat's claw extract, acai berry; and white willow bark extract is provided to a mammal to improve a variety of health related factors, including but not limited to brain health, joint health, eye health, mitondchorial optimization/improvement and reduction of inflammation and pain in a mammal.
US7329655 Drugs that inhibit phosphorylation kinases as an antigrowth or antiproliferation agent The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomeruloscierosis.
US20100204253 Ribosome Structure and Protein Synthesis Inhibitors The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism.
CN102000345A Complex folic acid/beta-cyclodextrin composite and preparation method thereof The invention discloses a complex folic acid/beta-cyclodextrin composite and a preparation method thereof. The composite is composed of beta-cyclodextrin and folic acid and the mass ratio of the beta-cyclodextrin to folic acid is 4-7:1. The preparation method comprises the following steps: adding weighted beta-cyclodextrin and folic acid into pure water for mixing to form suspension or solution; under the condition of heating and stirring, standing the reaction solution and cooling the solution until the solid material is sufficiently separated out and filtered; and drying a filter cake after the filtering to obtain the complex folic acid/beta-cyclodextrin composite. The invention has the advantages that the folic acid is embedded in a barrel hollow structure of the beta-cyclodextrin to be the folic acid-beta-cyclodextrin inclusion compound which has obviously enhanced stability, increased solubility and uninfluenced bioactivity; and the active ingredient, namely the folic acid, can be directly applied to foods, medicines and health care products in a clathrate compound mode, thereby overcoming the defects of poor stability, low water-solubility and the like.
CN102093191A Resveratrol chalcone derivative and preparation method thereof The invention discloses a novel resveratrol chalcone derivative for suppressing the proliferation of tumor cells. The general formula of the derivative is shown in the specifications, wherein R is shown in the specifications. The novel resveratrol chalcone derivative has a remarkable suppression effect on human oral cavity epicuticle tumor cell lines (KB) and human leukemia cell lines (K562), so that the novel resveratrol chalcone derivative can be applied to the preparation of anti-tumor medicaments. The invention also discloses a preparation method of the derivative.
CN102634561A Application of triptolide, triptolide derivant and triptolide analogue in preparation of antitumor drugs Application of triptolide, triptolide derivant and triptolide analogue in preparation of antitumor drugs relates to triptolide. A method for utilizing tRXRZ (truncated retinoid X receptor) alpha as a target spot to screen the triptolide, the triptolide derivant and the triptolide analogue which is tripdiolide includes a following step of acting the triptolide into a tumor cell line containing the tRXR alpha so as to obtain the triptolide, the triptolide derivant and the triptolide analogue which are screened by utilizing the tRXR alpha as the acting target spot. After the triptolide, the triptolide derivant and the triptolide analogue which are screened by utilizing the tRXR alpha as the acting target spot act to the tumor cell line, the tRXR alpha can be targeted, mutual actions of the tRXR alpha and p85 can be inhibited, then AKT (threonine kinase) activation induced by TNF (tumor necrosis factor) alpha can be inhibited, a caspase 8 apoptosis signal channel induced by the TNF alpha can be activated, and cancer cell apoptosis can be induced.
WO2006073835A3 Regiments for intra-articular viscosupplementation The invention provides viscosupplementation methods for treating osteoarthritis and joint injury with HA-based viscosupplements, particularly viscosupplements with an intra-articular residence half-life shorter than 3 weeks. Viscosupplements for use in the methods of the invention may be further characterized in that they contain less than 20 mg/ml HA, at least 5% (w/w) of which is in a gel form, such as, e.g., hylan B. In an illustrative embodiment, hylan G-F 20 (Synvisc®) is administered in a single intra-articular knee injection of 6 ± 2 ml.
CN101415417A Combination therapy of (2R,Z)-2-amino-2-cyclohexyl-N-(5-(1-methyl-1H-pyrazol-4-yl)-1-oxo-2,6-dihydro-1H-[1,2]diazepino[4,5,6-CD]indol-8-yl)acetamide The present invention relates to novel combination therapies of (2R,Z)-2-amino-2- cyclohexyl-N-(5-(1-methyl-1 H-pyrazol-4-yl)-1-oxo-2,6-dihydro-1 H-[1,2]diazepino[4,5,6-cd]indol-8- yl)acetamide (compound 1 ), a pharmaceutically acceptable salt or solvates thereof, or a mixture thereof, in combination with an anti-cancer agent or radiation therapy.
WO2007060976A1 Novel ascochlorin derivative compounds and medicinal compositions containing the same It is intended to provide an ascochlorin-related compound which is useful as a PPARϜ activator or a medicinal composition, in particular, a medicinal composition for preventing or treating life style-related diseases or preliminarily conditions thereof or a medicinal composition comparable to pioglitazone in preventing or treating type II diabetes, and the effective concentration of which in blood can be sustained for a certain period of time or longer but does not increase to the level of exerting toxicity; and a method of producing the same. Namely, an ascochlorin derivative compound represented by the general formula (I): [Chemical formula 10] (I) wherein R1 represents a hydrogen atom or -CnH2n+1 (wherein n is an integer of from 1 to 5); and R2 represents a hydrogen atom, -CnH2n+1 (wherein n is an integer of from 1 to 5), -CnH2nCOOR’ (wherein n is an integer of from 1 to 5; and R’ represents a hydrogen atom or a C1-3 alkyl group), or -COR” (wherein R” represents a pyridyl group, an amino group substituted by a C1-3 alkyl group, a phenoxyalkyl group having a halogen atom in its nucleus, a phenyl group having a C1-3 alkoxy group in its nucleus or a phenyl group having a C1-3 alkoxycarbonyl group in its nucleus); a pharmacologically acceptable salt thereof or a prodrug of the same.
CN103705813A Centipede anti-cancer pills The present invention provides a gastric cancer treatment technical scheme, which comprises a decoction and a powder drug, wherein the decoction comprises 10 g of hawthorn, 6 g of common burreed tuber, 10 g of milkvetch root, 15 g of upright ladybell root, 30 g of hematite, 30 g of common jujube, 30 g of dock root, 60 g of oldenlandia, 100 g of honeysuckle, 10 g of semen vaccariae, and 6 g of licorice root, and the powder drug comprises 30 g of panax notoginseng, 30 g of raw leech, 30 g of gecko, 30 g of raw pinellia, 30 g of centipede, 8 g of realgar, 25 mylabris, 30 g of ark shell, and 6 g of nux vomica. The centipede anti-cancer pills have effects of blood flow activating, blood stasis removing, diuresis inducing, edema alleviating, blood stasis dissipating, menstruation promoting, sore drawing, pus discharge, asthma stopping, vomit stopping, heat clearing, detoxification, swelling subsiding, pain relieving, poisoning treating through poisonous drugs, cancer cell inhibition, and cancer cell killing.
CA2303339C A pharmaceutical composition for treating dysmenorrhea and premature labor The present invention teaches a composition comprising a .beta.-adrenergic agonist in a bioadhesive carrier. Preferably, the composition comprises terbutaline in polycarbophil. The present invention additionally teaches the local administration of a .beta.-adrenergic agonist for the purpose of treating or preventing dysmenorrhea or premature labor. Using this composition and the method of treatment provides sufficient local levels of the drug to provide therapeutic efficacy, but avoids many untoward adverse events.
WO2009074020A1 Alpha-amino-n-substituted amides, pharmaceutical composition containing them and uses thereof Disclosed are α-amino-N-substituted amide compounds having the following structure or their pharmaceutically acceptable salts, and pharmaceutical compositions containing said compounds or their pharmaceutically acceptable salts. The present α-amino-N-substituted amide compounds or their pharmaceutically acceptable salts are anti-tumor and/or anti-cancer active in vitro and in vivo, can be effectively against various tumor and/or cancer cells, and they can therefore be used in the preparation of medicaments for the treatments tumor and/or cancer.
US20110201635 Substituted spiroindolinones There is provided a compound of the formula wherein X, Y, W, R1, R2 and R3 are as described herein. The compounds have activity as anticancer agents.
CN101724046A Human epididymis expression sperm binding protein HEL-18 and encoding gene and application thereof The invention belongs to biotechnology and medical field, and discloses a new human epididymis specific expression sperm binding protein HEL-18 and preparation and application thereof. The invention discloses an amino acid sequence of the HEL-18 protein and provides a recombination expression vector carrying a DNA sequence encoding the protein of the invention. The invention further discloses a method for preparing the protein and detecting the biological function of the HEL-6 protein. The protein has micro-expression in the epididymis, heart and lung tissue, and is combined with the back part of the head of the sperm, thereby playing an important role in fecundation, recognition and movement of the sperm. The HEL-18 protein can be used as target protein for the research and development of immunity acyeterion as well as clinical diagnosis and treatment of male infertility. The relevant gene or protein detecting method based on the protein HEL-18 can be widely applied to the reproductive medicine research field.
EP2320921A1 Compositions comprising tea tree oil and methods for the prevention and treatment of cancer Compositions for the treatment and/or prevention of cancer are described. Preferably the composition comprises a therapeutically effective amount of tea tree oil from Melaleuca alternifolia, together with a pharmaceutically or therapeutically acceptable carrier and/or diluent. Methods for the treatment and/or prevention of cancer are also described. Preferably the method is used for the treatment and prevention of skin cancer. More preferably, the method is used for the treatment and prevention of basal cell carcinoma, squamous cell carcinoma and/or melanoma.
US20050192266 Including vanadocene dihalides, bis(methylcyclopentadienyl), vanadocene diazide, vanadocene dicyanide, vanadocene dioxycyanate, vanadocene dithiocyanate, vanadocene diselenocyanate, vanadocene ditriflate, vanadocene monochloro oxycyanate, vanadocene monochloro acetonitrilo tetrachloro ferrate Novel spermicidal compounds which are organometallic cyclopentadienyl metal complexes, particularly vanadium IV complexes, are described including corresponding contraceptive and therapeutic compositions and method for providing contraception and selective killing of testicular germ cells. Included among the vanadium complexes are vanadocene dichloride, vanadocene dibromide, bis (methyl cyclopentadienyl) vanadium dichloride, vanadocene diiodide, vanadocene di-pseudohalides, and others. Most active found was vanadocene diselenocyanate.
US20110104308 Treatment For Diseases Relying On Discovery That Thioredoxin Mediates Nitric Oxide Patients having a disease associated with high level of thioredoxin system activity or a requirement for nitric oxide, e.g. large cell lymphoma or restenosis, are treated with a thioredoxin reductase inhibitor, e.g. auranofin or arsenic trioxide, and a nitric oxide donating compound, e.g. isosorbide mononitrite or isosorbide dinitrite or nitroglycerin or S-nittrosothiol. Patients having a disease associated with nitric oxide synthase overexpression or increased activity, e.g. Parkinson's disease or septic shock or pancreatic cancer, are treated with Trx/Trx reductase upregulator, e.g. aptamer that binds to thioredoxin reductase inhibitor, and agent causing depletion of nitric oxide (or adduct thereof), e.g. L-NMMA or L-NAME or minocycline or ascorbate or N-acetylcysteine.
WO2009111279A1 Pyrazole [3, 4-b] pyridine raf inhibitors Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
EP2608792A1 Methods of administering an egfr inhibitor Disclosed are methods of treating a patient having cancer with an EGFR inhibitor requiring an active step of avoiding or modifying the co-administration of such drugs with P-gp modulators. This invention also relates to a medicament for treating a patient having cancer, comprising an EGFR inhibitor as the active product ingredient, customized for avoiding co-administration with P-gp inducers and/or inhibitors by an instruction added to the medicament or the package containing said medicament.
CA2177827C Novel apoptosis-modulating proteins, dna encoding the proteins and methods of use thereof The present invention provides a novel family of apoptosis-modulating proteins. Nucleotide and amino acid residue sequences, derivatives thereof and methods of use thereof are also provided.
US20090048222 Triaza Compound Immunoregulatory Agents The invention provides certain macrocyclic triaza compounds which down-regulate CD4 expression for use in the treatment of autoimmune diseases and inflammatory diseases or conditions. In a specific embodiment, the invention provides certain naphthalene substituted triaza macrocycles which exhibit high activity for down regulation of CD4 expression. In particular, triaza macrocycles having dansyl groups are provided for use in pharmaceutical compositions.
US20110230505 Quinazoline inhibitors of bace 1 and methods of using Dihydroquinazoline compounds, compositions containing them, the use of the compounds and compositions for the treatment of Alzheimer's disease are described.
EP1257277B1 New drug combinations comprising a norepinephrine reuptake inhibitor and an antimuscarinic agent A composition comprising: (a) a pharmaceutically effective amount of one or more norepinephrine reuptake inhibitors or a pharmaceutically effective salt thereof; and (b) a pharmaceutically effective amount of one or more antimuscarinic agents or a pharmaceutically effective salt thereof is provided. The composition is useful in treating disorders or diseases of the central nervous system, and particularly useful in treating incontinence.
CN103417502A Hydrogen sulfate clopidogrel tablet and preparation method thereof The invention relates to a hydrogen sulfate clopidogrel tablet and a preparation method thereof. The method comprises the following steps: firstly, preparing hydrogen clopidogrel and hydroxy propyl cellulose into micro-capsules by utilizing a drying-in-liquid method, then mixing with common auxiliary material in pharmacy, and preparing the tablet by tabletting.
US6888015 Sphingolipid synthesis inhibitor A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16. (in the formula, X is an aliphatic alkyl group, desirably is an aliphatic alkyl group having 7 to 15 carbon atoms).
EP2598480A1 Cyclopropylamine derivatives useful as lsd1 inhibitors The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
US20060104925 Particle comprising a host lattice and a guest, its preparation and use in ultraviolet light screening compositions A UV screening composition comprising novel particles which are capable of absorbing UV light so that electrons and positively charged holes are formed within the particles is disclosed. These particles comprise a host lattice incorporating a second component to provide luminescence trap sites and/or killer sites, said second component being niobium, vanadium, antimony, tantalum, strontium, calcium, magnesium, barium, molybdenum or silicon.
CN102225064A Application of isoflavone compound in preparing medicines for treating radiation injuries The invention relates to an application of an isoflavone compound in preparing medicines for treating radiation injuries. In vivo/in vitro experiments prove that the compound has the advantage of low systematic toxicity, and when the effective dose for treating radiation injuries is applied, the compound can not induce loss of body weight and systematic toxicity, especially toxicity to a reproductive system.
EP1790636A1 Piperidine derivatives and use thereof The present invention provides a compound represented by the formula: wherein Ar is an aryl group optionally having substituents, R is a C1-6 alkyl group, R1 is a hydrogen atom, a hydrocarbon group optionally having substituents, an acyl group or a heterocyclic group optionally having substituents, X is an oxygen atom or an imino group optionally having substituents, ring A is a piperidine ring optionally further having substituents, and ring B is a benzene ring having substituents, or a salt thereof, and an agent for the prophylaxis or treatment of lower urinary tract abnormality and the like, which contains the compound.
WO2008086069A1 Methods of treating itch The invention provides methods for preventing and/or treating itch in a subject in need thereof by administration of a protease- activated G-protein coupled Protease Activated Receptor 4 (PAR4) antagonist. The PAR4 antagonist can be combined with a PAR2 antagonist.
CN101463055B O-indican compounds, preparation and use thereof The invention relates to the medicine field related to diabetes, in particular to O-glycoside which has therapeutic action on the diabetes and is taken as a sodium glucose transporter 2 (SGLT2) inhibitor, a preparation method and application thereof to preparing a diabetes drug, wherein, groups are defined as the specification.
US20130045290 Dermal rejuvenation compositions and methods The present invention relates, e.g., to a system for treating damaged skin, comprising a cosmeceutical formulation comprising about 1-10% of a mixture of perfluorocarbons (PFC's) of at least three different molecular weights, and about 0.001-5% hyaluronic acid (HA) of molecular weight about 100 kDa or less, packaged in an aerosol spray container.
CN101053569A Bismuth glycyrrhizate capsule and its preparation The invention provides a new medical preparation bismuth glycyrrhetate capable of treating stomach and duodenum abscess and preparation method thereof. The purpose of the invention is to complement the current techniques and provides a capsule which is characterized in simple oral-taken, capable of concealing medical peculiar smell, easy taking and good for improving stability of the product. The invention also creates in the preparation method of the raw materials, which has the features of simple process, easy control, stable product quality and suitable for the current large-amount of production etc.
EP2374449A2 Composition including at least one aqueous phase and at least one oil phase including ivermectin Composition comprises a fatty phase, an aqueous phase and a compound of avermectin family, where the fatty phase comprises an oily solvent different from mineral and vegetable oils, in which the avermectin compound is solubilized. An independent claim is included for the preparation of the composition comprising mixing ivermectin with an oily solvent, until ivermectin is solubilized, to form the fatty phase, mixing constituents of the aqueous phase, up to homogeneity and incorporating the fatty phase in the aqueous phase to form an emulsion. - ACTIVITY : Dermatological; Antiseborrheic. - MECHANISM OF ACTION : None given.
WO2006108789A1 Novel enantiomers and their use as monoamine neurotransmitter re-uptake inhibitors This invention relates to novel enantiomers of Formula I useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
US20100160394 Use of 4-[(4- thiazolyl)phenoxy]alkoxy-benzamidine derivatives for the prophylaxis and treatment of osteoporosis This invention relates to a pharmaceutical composition containing 4-[(4-thiazolyl)phenoxyl]alkoxy-benzamidine derivatives expressed by the following formula 1 for the prophylaxis and treatment of osteoporosis and more particularly, to the use of 4-{5-[4-(5-isoproply-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine or N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine expressed by the following formula 1 as a pharmaceutical composition for the prophylaxis and treatment of osteoporosis.
WO2014082569A1 Use of artemether in preparation of drug for treating leukemia Disclosed is a use of artemether in the preparation of a drug for treating leukemia. The drug is an artemether injection or lyophilized injection, and is prepared with the artemether and a water soluble cyclodextrin derivative in a weight ratio of 1: 30-70.
WO2009136995A3 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods ofinhibilion the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as cardiovascular disease, inflammatory disease and autoimmune disease and cell proliferative disorder. Formula (I) Y1 is selected from the group consisting of: (a) and (b); Z is O or S; D1 is selected from the group consisting of: (a) phenyl substituted with a group, R5 (b) naphthyl (c) C3-8cycloalkyl (d) heteroaryl (e) heterocyclyl
CN103638419A Washing liquor for treating eczema The invention relates to washing liquor for treating eczema. The washing liquor comprises the following components in parts by weight: 40 to 50 parts of fructus cnidii, 40 to 50 parts of honeycomb, 40 to 50 parts of calomel, 20 to 30 parts of kadsura pepper stem, 20 to 30 parts of herba siegesbeckiae, 20 to 30 parts of phaseolus calcaratus, 20 to 30 parts of alpinia katsumadai, 10 to 20 parts of liquorice, and 5 to 10 parts of cassia twig, wherein the fructus cnidii is used for relieving itching, and dispelling wind and eliminating dampness; the honeycomb has the effects of counteracting toxic substances and eliminating worms, dispelling wind, and relieving itching; the calomel has the effect of counteracting toxic substances; three medicines are combined to use as major medicines; the kadsura pepper stem has the effects of expelling wind-damp, and dredging channel; the herba siegesbeckiae has the effects of dispelling wind and eliminating dampness, clearing and activating the channels and collaterals, and clearing away heat and toxic materials; the phaseolus calcaratus has the effects of resolving toxin and expelling pus; the alpinia katsumadai has the effect of eliminating dampness and promoting circulation of Qi; the four medicines are combined to use as auxiliary medicines; the cassia twig has the effect of warning channel and dredging arteries and veins. The nine medicines are combined to use and can effectively treat eczema. The washing liquor has the advantages of rational formula, is capable of dispelling wind, relieving itching, detoxifying and eliminating dampness, and low in side effect, and can effectively treat eczema.
US20090036453 Pyrrolopyridazinone Compound The present invention discloses a pyrrolopyridazinone compound represented by the formula (1): wherein R1 represents C1-C2 alkyl group or halogeno C1-C2 alkyl group, R2 repersents C3-C5 cycloalkyl group, (C3-C5 cycloalkyl)C1-C2 alkyl group or C1-C3 alkyl group, R3 represents hydrogen atom, or methylene group or cis-vinylene group for forming substituted oxygen-containing hetero ring in combination with group —O—R2, R4 represents hydrogen atom, halogen atom, C1-C8 alkyl group, C2-C6 alkenyl group, C2-C6 alkynyl group, hydroxy C3-C6 alkenyl group, hydroxy C3-C6 alkynyl group, C1-C6 alkyl group substituted by substituent(s) selected from Substituent group (a), C3-C6 cycloalkyl group which may be substituted by substituent(s) selected from Substituent group (b), “C1-C3 alkyl group which is substituted by C3-C6 cycloalkyl group which may be substituted by substituent(s) selected from Substituent group (b), and which may be substituted by a hydroxy group”, an aromatic ring group or heteroaromatic ring group each of which may be substituted by a substituent(s) selected from Substituent group (c) or “C1-C2 alkyl group which is substituted by aromatic ring group or heteroaromatic ring group each of which may be substituted by group(s) selected from Substituent group (c), and which may be substituted by a hydroxy group”, Substituent group (a) represents a halogen atom, hydroxy group, cyano group, carboxy group, C1-C5 alkoxy group, halogeno C1-C4 alkoxy group, C3-C6 cycloalkoxy group, (C3-C6 cycloalkyl)C1-C2 alkoxy group, C1-C4 alkoxycarbonyl group, C2-C4 alkanoyl group, C2-C4 alkanoyloxy group or C1-C4 alkyl-substituted amino group, Substituent group (b) represents a hydroxy group or a halogen atom, Substituent group (c) represents a halogen atom, a hydroxy group, a cyano group, a nitro group, a carboxy group, C1-C5 alkoxy group, C1-C4 alkoxycarbonyl group, C2-C4 alkanoyloxy group, C1-C4 alkyl-substituted amino group or a C1-C4 alkyl group which may be substituted by a substituent(s) selected from the group consisting of (a halogen atom, a hydroxy group and a carboxy group), or a pharmaceutically acceptable salt thereof.
WO2010142642A1 4 -hydrazono- 1,4 -dihydropyridine derivatives for the treatment of neurodegenerative diseases The present invention relates to pharmaceutical compositions comprising pyridinylidene hydrazone derivatives and their uses in the treatment or prevention of neurological and/or neurodegenerative disorders and/or diseases such as, e.g., Alzheimer's disease. Down's syndrome, Hereditary cerebral hemorrhage with amyloidosis Dutch type, Parkinson's disease, ALS (amyotrophic lateral sclerosis). Creutzfeldt-Jacob disease, Huntington's disease, HIV- related dementia, Lewis body dementia and motor neuropathy.
WO2006038797A1 Use of statin or precursor thereof for the treatment of hiv infections The invention relates to a new use of statins. It was found that statins are capable of reducing human immunodeficiency virus (HIV) infection of cells that are normally susceptible to HIV-infection. Provided are pharmaceuticals, methods and uses of a statin in the treatment of infections.
EP1693384A2 Functional immunoglobulins against human serum albumin, fragments thereof, library thereof and methods of production thereof The present invention relates to functional immunoglobulin variable domains or antigen-binding fragments thereof that bind human serum albumin. It further relates to variants thereof, artifiical mutants, vectors, hosts cells and methods of preparation.
WO2014032099A1 Composition and method for bone growth A composition for promoting bone growth comprising a sugar based high viscosity carrier, such as sucrose acetate isobutyrate (SAIB); an osteoinductive agent, such as bone morphogenetic protein; an anti-resorptive agent, such as bisphosphonate; and optionally an osteoconductive agent, such as hydroxyapaptite.
CN1879708A A hicismus-treating medicine with aucklandia root Disclosed is a medicament for treating body odor, which is prepared from banksia rose, broom cypress fruit, green copperas, lead monoxide, perfume compound and ethanol through the steps of disintegrating, sieving, mixing and immersing.
CN101272782B Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).
WO2010108855A1 5-β, 14-β-ANDROSTANE DERIVATIVES USEFUL FOR THE TREATMENT OF PROTEINURIA, GLOMERULOSCLEROSIS AND RENAL FAILURE Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/or treatment of proteinuria, glomerulosclerosis or renal failure.
US6960585 For therapy of inflammatory and immune diseases Compounds of formula (I), or pharmaceutically-acceptable salts thereof, are useful in treating inflammatory and immune diseases and disorders, wherein X, Y1, Y2, and R2- 4 are as defined in the specification.
WO2007088343A8 Granular material comprising water- insoluble inorganic phosphate binders There is provided a granular material comprising (i) at least 50 % by weight based on the weight of the granular material of solid water-insoluble mixed metal compound capable of binding phosphate of formula (I): MII1-XMIIIX(OH)2An-y.ZH2O (I) where MII is at least one of magnesium, calcium, lanthanum and cerium; MIII is at least iron(lll); An- is at least one n-valent anion; x = ∑ny; 0 < x ≤ 0.67, 0 < y ≤ 1, and 0 ≤ z < 10; (ii) from 3 to 12 % by weight based on the weight of the granular material of non-chemically bound water, and (iii) no greater than 47 % by weight based on the weight of the granular material of excipient.
WO2011018894A1 Pyrrolopyrimidine derivatives as potassium channel modulators The present invention relates to pyrrolopyrimidine derivatives of formula(I). They have activation activities of potassium channels as the SK channels, and are useful in the treatment or prevention of disorders and diseases in which potassium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which potassium channels are involved. The present invention also relates to the prevention or treatment of such diseases, which comprises administering the above-mentioned pyrrolopyrimidine derivatives to a subject in need of such a prevention or treatment a therapeutically effective amount of said derivative.(I) (R1=Hydrogen etc, R2=Hydrogen etc, R3=C1-6alkyl etc, R4= Hydrogen etc, n=1-4)
EP2292590A2 Prodrugs of 9-aminomethyl tetracycline compounds A compound of the formula (II): wherein Q' is a prodrug moiety or a pharmaceutically acceptable salt thereof.
WO2014116849A1 Crystalline forms of {[1-cyano-5-(4-chlorophenoxy)-4-hydroxy-isoquinoline-3-carbonyl]-amino}-acetic acid The present disclosure relates to crystalline forms of {[1-cyano-5-(4-chlorophenoxy)-4-hydroxy-isoquinoline-3-carbonyl]-amino}-acetic acid (Compound A), the process of preparing crystalline forms of Compound A, the pharmaceutical compositions containing them, and the methods of use thereof.
WO2011047515A1 Indenoisoquinolinone derivatives, manufacturing method and medical use thereof. Indenoisoquinolinone derivatives (I), the manufacturing method and the medical use thereof, which belong to pharmaceutical chemistry and organic chemistry field, are disclosed. These compounds can be used for treating several medical symptoms related to postmenopausal syndrome, uterine fibers deterioration and aortic smooth muscle cells proliferation, especially ER-(+) depend breast cancer. Meanwhile, these compounds can also be used for treating glioma and lung cancer, and have inhibiting effect on tumor metastasis.
WO2014023754A1 Compounds for use in the treatment of disorders that are ameliorated by inhibition of hdac The present invention relates to compounds of formula (I) and (IV), and pharmaceutically acceptable salts, tautomers, stereoisomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are for usein the treatment of disorders that are ameliorated by inhibition of HDACsuch ascancer and hemoglobinopathieslike β-thalassemia or sickle cell anemia.
CA2853732A1 Nonaqueous compositions for bone hemostasis, and methods for their use and manufacture Bone hemostat compositions, and methods for their use and manufacture are provided. Exemplary hemostatic compositions include polymeric components such as random and non-random copolymers, natural polymers, ceramics, reactive group polymers, and combinations thereof. Bone compositions may be used during surgical procedures, and may be applied to bone to inhibit or prevent bleeding from bone.
CN1769268A Use of natural or artificial isorhodanate analog compound JC-5411 in preparing transcription factor SP1 inhibitor The invention relates the isosulfocyanate compounds (ISOTHIOCYANATES), in other word, JC-5411 compounds, which can adjust the expression of androgen acceptor gene in cell by suppressing the expression of gene transcription factor SP1, and suppress the abnormal breeding function of prostate gland cell. With the little compound, it can suppress hamster benign hypertrophy of the prostate (BPH), which is induced by suppressed male sex hormone, and the growth of prostate gland cancer cell. The invention provides the new method of effectively preventing and treating the hypertrophy of the prostate and prostate gland cancer. The compound possesses the low side effect, steady chemical biology nature, low cost of manufacture, and broad adaptability.
US7202044 Method for detecting a progressive, chronic dementia disease, and corresponding peptides and detection agents The invention relates to defined peptides and the quantitative determination thereof in body fluids of patients suffering from progredient chronic dementia, in relation to the concentration of said peptides in a control group. The inventive peptides come from a protein precursor having the corresponding gene, are processed in a specific manner, and are optionally post-translationally modified, especially phosphorylized. An increase in the concentrations of these peptides or the corresponding non-processed protein indicates progredient chronic dementia. Progredient chronic dementia is detected by identifying the peptides and/or the protein individually or in combinations. The invention also relates to the use of said peptides for controlling the course of progredient chronic dementia and for the prognosis of progredient chronic dementia, especially for complementing or replacing mini-mental scores, and for developing therapeutic agents to combat progredient chronic dementia such as Alzheimer's disease.
CN101766580A Scopoamine butylbromide ibuprofen tablet and preparation method thereof The invention discloses a scopoamine butylbromide ibuprofen tablet and a preparation method thereof. The preparation is made of ibuprofen, scopoamine butylbromide and effective auxiliary materials in pharmaceutics by adopting granulation tabletting through a direct tablet compressing method or a wet method. The invention has the advantages of rapid effect for relieving pain and obvious analgesia effect, and can be widely used for relieving moderately severe pain, in particular severe pain.
CN102973592A Application of dextran sulfate in preparing medicament for treating diabetes mellitus The invention discloses novel application of dextran sulfate in preparing a medicament for treating diabetes mellitus. The medicament can protect a body from insulin resistance due to chronic inflammation caused by activated macrophage generated by fat and other reasons, so that attack or symptom worse of diabetes mellitus. Dextran sulfate has good curative effect in a high glucose and lysophosphatidylcholine induced animal model; and the medicaments used in the application can be easily acquired, low in price and stable in properties, are convenient to store and transport, and have wide application prospect.
CN102793732A Medical biological hemostatic gel and preparation method thereof The invention discloses medical biological hemostatic gel which comprises the following components in percentage by weight: 1 to 1.5 percent of water-soluble chitosan, 0.5 to 1 percent of pseudo-ginseng powder, 0.2 to 0.3 percent of chlorhexidine acetate, 1 to 1.5 percent of carbomer, and 95.7 to 97.3 percent of deionized water. A preparation method of the medical biological hemostatic gel comprises the following steps of: 1, heating the deionized water to a temperature of between 55 and 60 DEG C; 2, adding the chlorhexidine acetate, and stirring and dissolving; 3, adding the water-soluble chitosan, and stirring for dissolving; and 4, adding the pseudo-ginseng powder and the carbomer, stirring for dissolving, and cooling to room temperature to prepare the medical hemostatic gel. The using method of the biological hemostatic gel is as follows: directly applying the biological hemostatic gel to the injury, so that the effects of quickly stopping bleeding, sterilizing, promoting healing and reducing skin scars can be achieved.
US20060057252 Composition containing calcium pantothenate and vitamin A composition containing calcium pantothenate and at least one kind of vitamin as a mixture of solid state, wherein the calcium pantothenate is crystalline calcium pantothenate obtainable by a method comprising the following steps: (1) the step of mixing crystalline calcium pantothenate and amorphous calcium pantothenate to prepare a homogenous mixture; (2) the step of allowing the homogenous mixture obtained in the aforementioned step (1) to absorb moisture to prepare crystalline calcium pantothenate; and (3) the step of repeating the aforementioned steps (1) and (2) by using the crystalline calcium pantothenate obtained in the aforementioned step (2), and having a ratio (I16.0/I5.1) of the diffraction intensity I16.0 at an diffraction angle (2 θ) of 16° relative to the diffraction intensity I5.1 at an diffraction angle (2 θ) of 5.1° of 1 or more in a powder X-ray diffraction pattern.
US20060235076 Medicinal composition for treating infection with drug-resistant staphylococcus aureus The invention relates to a therapy of an infection with a drug resistant bacterium wherein a characteristic of multivalent phenol derivatives and/or extracts from “Tara” which enhance the activity of β-lactam antibiotics on the drug resistant bacteria is utilized. Specifically, the invention relates to an enhancer of β-lactam antibiotics comprising a multivalent phenol derivative or its pharmaceutically acceptable salt, a pharmaceutical composition comprising a β-lactam antibiotic and a multivalent phenol derivative and/or extract from “Tara” for the therapy of an infection with a drug resistant bacterium, a disinfectant for the same, and a functional food comprising a multivalent phenol derivative and/or extract from “Tara”.
CN101513427A Use of epimedin C The invention discloses use of epimedin C in preparing medicament for treating osteoporosis. In examination, under equal dosage, effect of the epimedin C is better than that of epimedium, epimedum total flavone and icariin, and the epimedin C can be used for preparing medicament for treating osteoporosis. Compared with the prior art, under equal dosage, effect of the epimedin C is better than that of epimedium, epimedum total flavone and icariin in treating osteoporosis, and effect of compound medicament of the epimedin C and other medicament (such as estrogen) is better than that of compound medicament of epimedum total flavone and same medicament. Under equal dosage, active component of the epimedin C is higher, and the invention provides a medicament selection with better curative effect for treating osteoporosis.
CN103404515A Method for preparing compound macranthoinG and application of compound in preparation of antibacterial agent The invention discloses a method for preparing a compound macranthoinG and application of the compound in preparation of an antibacterial agent. According to the method, the alien invasive plant crofton weed which is widely distributed in China is adopted as a raw material to extract and separate a high-bioactivity antibacterial agent (medicine) macranthoinG, and the source of the plant material is very wide, and prevention and control on further invasion and expansion of the crofton weed can be promoted by massively collecting and utilizing the crofton weed material during the application and development, so that the method has excellent potential economic and ecological benefits.
CN1742711A Menantine hydrochloride effervescent tablet and preparing method thereof The present invention relates to a memantine hydrochloride effervescent tablet for curing senile dementia and its preparation method. It is made up by using memantine hydrochloride as raw material and adding a certain auxiliary material according to conventional process.
EP1861391B1 Methods for preparing substituted sulfoxide compounds Disclosed are an optically pure compound having formula (I), its pharmaceutically acceptable salt and its pharmaceutically acceptable solvate, and a use thereof in manufacturing medicaments and pharmaceutical compositions. A process for preparing the compound defined therein is also provided. Formula (I).
US20110269762 Methods for treating atrial fibrillation and reducing stroke rate in atrial fibrillation patients The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering budiodarone to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of budiodarone and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of budiodarone may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling. In some methods of the invention, budiodarone is administered 400 mg BID or more preferably 600 mg BID.
US20070264211 Composition Comprising Sodium Silicate for Use in the Treatment of Dry Skin Conditions A composition contains sodium silicate and is used in the treatment of dry skin conditions, inter alia psoariasis, dermatitis and eczema. The composition is formulated into creams, ointments and sprays, each formulation being adapted to the intended skin application area.
CN101791412A Acyclovir-chitosan-stearic acid grafting, synthetic method and application thereof The invention provides a hydrophilic antiviral drug, namely acyclovir-chitosan-stearic acid grafting, which is beneficial to the load of the drug by a target carrier material through chemical grafting by the synthesis of an acyclovir-succinic acid midbody. On the basis, by adopting the load of the antiviral drug in cells of a molecular target mark for a chitosan-stearic acid grafting micelle with high-efficiency cellular uptake and low toxicity, the drug uptake of virus cells is greatly increased, and the drug concentration of the drug molecular target mar position is increased. The acyclovir-chitosan-stearic acid grafting increases the drug uptake of virus cells, is beneficial to reducing the distribution of the drug in normal tissues or cells and reduces the toxic side effect of the drug; and the drug concentration increase of the drug molecular target mark position is beneficial to increasing the healing effect of the antiviral drug. The acyclovir-chitosan-stearic acid grafting has the chemical general formula (disclosed in the specification).
US20110053934 Compounds and methods of treatment A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity.
WO2008047983A1 Composition for preventing and treating inflammatory bowel diseases In the inflammatory bowel diseases, guggulsterone (or a derivative thereof) extracted from C. mukul intercepts lkB kinase of the bowels irritated by LPS or lL-1β to inhibit inhibits NF-kB activation, thereby reducing inflammation response. Also, the pharmaceutical composition may be advantageously used without side effects, since it contains a substance extracted from a plant.
US20090202633 Extended release formulations of guaifenesin The present invention relates to extended release formulations comprising expectorant. More particularly, the present invention relates to extended release formulations comprising guaifenesin. The present invention also relates to a process for the preparation of extended release formulations comprising guaifenesin.
CN102617536A Isoflavone compound, its preparation method, and its application in preparation of antiviral or antitumor drugs The invention relates to an isoflavone compound, its preparation method, and its application in the preparation of antiviral or antitumor drugs, and concretely relates to a compound with a structural formula represented by formula (I). In the formula (I), R1 is hydrogen or C1-6 alkyl; X is -O-, -NH-, -CH=CH-, or ethinyl, or R2 is directly connected with benzopyran; R2 is selected from substituted or unsubstituted phenyl, substituted or unsubstituted heteroaryl, C1-16 alkyl, C1-16 alkyloxy, C1-16 alkyloxycarbonyl, or substituted or unsubstituted benzoyloxy; the heteroaryl is selected from groups derived from a five or six-membered heterocycle or a fused heterocycle containing one or two hetero atoms of N, O or S, and is selected but not limited to pyridyl, benzopyridyl, or groups derived from phenoxathiin, thiophene, oxazole and benzopyridine; and above substituent is selected from halogen, cyan, nitro, hydroxy, amino, C1-6 monosubstituted or disubstituted amino, C1-16 alkyl, halogenated C1-6 alkyl, C2-6 alkenyl, C6-12 arylalkenyl, C1-16 alkyloxy, C1-16 carboxyl, C1-16 alkyloxycarbonyl, C1-16 alkylcarbonyl, and substituted or unsubstituted phenoxyl. The invention also provides the preparation of the compound.
EP1207891B1 Use of a low molecular weight sulphated polysaccharide in the treatment of thrombosis The invention concerns the use of a sulphated polysaccharide capable of being obtained by radical depolymerization of a raw fucan derived from Pheophyceae, said polysaccharide having a molar mass not more than 10.000 g/mol, to obtain a medicine for preventing or treating vascular thrombosis, in particular venous thrombosis, arterial thrombosis and arterial restenosis.
EP1970047A1 Polyaphron topical composition with a corticosteroid A topical composition comprising a continuous phase and at least one discontinuous phase, said composition comprising at least one polyaphron dispersion and at least one corticosteroid and said continuous phase comprising 0 to 60% by weight of a C1 - C4 alcohol, ethylene glycol, a liquid polyethylene glycol, propylene glycol, a liquid polypropylene glycol, diethylene glycol mono ethyl ether or mixtures thereof.
CN102670556A Tacrolimus osmotic pump type controlled release tablet The invention provides a novel tacrolimus osmotic pump type controlled release tablet, which adopts ethyl cellulose and polyvinylpyrrolidone as semipermeable membrane formation materials, an asymmetric tablet type is preferable, the ageing phenomenon of the semipermeable membrane can be overcome, and the medicine residue is lowered. The invention also provides a method for improving the anti-ageing performance of the tacrolimus osmotic pump type controlled release tablet. The method is characterized in that the ethyl cellulose-polyvinylpyrrolidone is adopted to serve as the semipermeable membrane material. In addition, the invention also provides an application of the ethyl cellulose-polyvinylpyrrolidone composite to prepare the tacrolimus osmotic pump type controlled release tablet with the anti-ageing performance.
WO2008135984A1 Composition comprising s-allylmercapto-n-acetylcysteine (assnac) for up-regulation of cellular glutathione level The present invention relates to S-allylmercapto-N-acetylcysteine (ASSNAC) and its pharmaceutically acceptable salts and solvates, which are useful for up-regulation of cellular glutathione levels and expression of phase II detoxifying enzymes. The invention further provides methods of use thereof in the prevention, alleviation or treatment of oxidative stress induced by reactive oxygen species (ROS).
US20130023574 Method for generating data set for integrated proteomics, integrated proteomics method using data set for integrated proteomics that is generated by the generation method, and method for identifying causative substance using same Provided are a method for generating a data set for integrated proteomics analysis, whereby expression level variations of both of proteins and genes can be integrally united together and, moreover, highly accurate and appropriate analysis results can be obtained compared with the existing cases where the expression variation amount of proteins or genes is singly analyzed, an integrated proteomics analysis method, a method for identifying a protein causative of a disease or the like using these methods, and a method of using the same???. The aforesaid method for generating a data set for integrated proteomics analyses comprises: a protein identity number-assigning step for assigning common identity numbers to the expression variation amount data of individual proteins; a gene identity number-assigning step for assigning common identity numbers to the expression variation amount data of individual genes; a data-binding step for binding together the set of the expression variation amount data; a data-rejecting step for rejecting, among the individual expression variation amount data constituting the thus bound data set, data showing a p-value equal to or greater than a specific level; and a data-selecting step for selecting one data, from a set of data having the same common identity number assigned thereto, on the basis of a definite requirement to thereby generate the data set to be subjected to integrated proteomics analyses. Further, the data set for integrated proteomics analyses thus generated is subjected to GO analysis and network analysis to thereby identify a protein causative of a disease, a pathological condition or the like. Furthermore, the causative protein thus identified is usable, for example, a tumor marker or a clinical target.
CN102166223A Composition for treating streptococcus suis and method for preparing composition The invention discloses a composition for treating streptococcus suis and a method for preparing the composition and aims to provide the composition which can treat streptococcus suis, is convenient to use and address both the symptoms and root causes and a method for preparing the composition. The composition comprises the following components in percentage by weight: 3 to 10 percent of amoxicillin, 5 to 15 percent of sulphadiazine sodium, 1 to 3 percent of lactic acid TMP, 5 percent of sodium carbonate, 5 to 15 percent of sodium bicarbonate, 5 to 15 percent of paracetamol and the balance of anhydrous glucose. Because the amoxicillin and the sulphadiazine sodium are used as anti-pathogenic ingredients, the pathogenic sensitivity is improved, the probability of causing drug resistance is lowered, the secondary bacterial infection can also be treated, the lactic acid TMP has obvious synergism on the amoxicillin and the sulphadiazine sodium, and the anti-disease ability is improved; the sodium carbonate has the solubilization effect on amoxicillin and sulphadiazine sodium, so that the product is soluble in water and can be taken by water drink; and the sodium bicarbonate can lower the side effects of sulphadiazine sodium and prevent the generation of crystalluria, and the paracetamol has the effects of quickly removing heat and resisting inflammation.
CN103483462A Preparation method for phascolosoma esculenta polysaccharide and application of phascolosoma esculenta polysaccharide in treating septicemia The invention discloses a preparation method for a phascolosoma esculenta polysaccharide and application of the phascolosoma esculenta polysaccharide. Endogenous enzyme killing is firstly performed on phascolosoma esculenta power, then enzymolysis is performed on the phascolosoma esculenta power through a combined enzyme formed by subtilisin and Alacase protease, and after tri-filtering on the enzymatic hydrolysate, the phascolosoma esculenta polysaccharide is obtained through vacuum concentration and drying. The preparation method has the advantages that the preparation is simple, the deproteinization process and the ethyl alcohol precipitation process are eliminated, the production period is shortened, energy conservation, emission reduction and environment protection are facilitated, the enzymolysis effect is still good, and the content of polysaccharide in the phascolosoma esculenta polysaccharide can reach 50 to 70 percent. The phascolosoma esculenta polysaccharide has the effect of resisting septicemia.
US7091372 Process for the preparation of 1,3-substituted indenes and aryl-fused azapolycyclic compounds The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: wherein R1, R2, R3, R4, and R5 are defined herein. Compounds of formulae (Ia), (Ib) and (Ic) or mixtures thereof are useful in the preparation of compounds of formula (II): wherein R2, R3 and R6 are also defined herein.
US20080176882 Salts of 3-(3-amino-2-(r)-hydroxy-propyl)-1-(4-fluoro-phenyl)-8-(8-methyl-naphthalen-1-ylmethyl)-1,3,8-triaza-spiro[4.5]decan-4-one The present invention is directed to salts of 3-(3-amino-2-(R)-hydroxy-propyl)-1-(4-fluoro-phenyl)-8-(8-methyl-naphthalen-1-ylmethyl)-1,3,8-triaza-spiro[4.5]decan-4-one, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by NOP, for example depression, anxiety, alcohol abuse, etc. The present invention is further directed to process(es) for the preparation of 3-(3-amino-2-(R)-hydroxy-propyl)-1-(4-fluoro-phenyl)-8-(8-methyl-naphthalen-1-ylmethyl)-1,3,8-triaza-spiro[4.5]decan-4-one and its corresponding salts.
WO2011066735A1 An Amorolfine HCl Crystal and the Preparation thereof This invention relates to an Amorolfine HCl crystal, to its preparation, to its use in the preparation of antifungal drugs and to a pharmaceutical composition containing the Amorolfine HCl crystal.
CA2487365C Piperidine derivatives as potassium channel blockers The invention provides compounds of formula: (see formula I) wherein: m is 0, 1 or 2; each R1 independently represent halogen or cyano; and R2 represents H or CH3, or a pharmaceutically acceptable salt thereof. The compounds and compositions containing them are useful for the treatment of human diseases or conditions in which modulation of chemokine receptor activity is beneficial, e.g., rheumatoid arthritis, chronic obstructive pulmonary disease, asthma or multiple sclerosis.
US20130171232 Heat Patch for Parkinson's Disease Provided in the present invention are a composition for treating or ameliorating Parkinson's and methods of making and using the same.
CN103288818A Anti-cancer drug based on benziso-selenazolone as well as preparation method and application thereof The invention relates to an anti-cancer drug based on benziso-selenazolone, in particular to a 2-(2-substituted benxoyl methylthio-1,3,4-thiadiazole-5-yl)-benziso-selenazolone derivative. The preparation method disclosed by the invention comprises the following steps of: taking 2-chloride selenium benzoyl chloride as the raw material; carrying out condensation reaction with 1,3,4-thiadiazole derivative in acetonitrile solvent; then, preparing a target object. The preparation method disclosed by the invention can be used for preparing anti-tumour pharmaceutical compositions. The anti-cancer drug based on benziso-selenazolone disclosed by the invention has the advantages that the structure is confirmed through infrared spectroscopy, H nuclear magnetic resonance, element analysis and the like; inhibitory activities of human breast cancer cells, liver cancer cells and lung cancer cells are tested; the result shows that a series of derivatives has better inhibitory effects on human breast cancer cells MCF-7, human liver cancer cells SMMC-7721 and human lung cancer cells A549, and therefore, the anti-cancer drug based on benziso-selenazolone disclosed by the invention has potential application prospect.
US6995269 Guanidinobenzamides Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
WO2005101004A3 Diagnostics and therapeutics for diseases associated with purinoceptor 1 type y (p2y1) The invention provides a human P2Y1 which is associated with the cardiovascular diseases, dermatological diseases, endocrinological diseases, metabolic diseases, inflammation, gastroenterological diseases, cancer, hematological diseases, respiratory diseases, muscle skeleton diseases, neurological diseases and urological diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular diseases, dermatological diseases, endocrinological diseases, metabolic diseases, inflammation, gastroenterological diseases, cancer, hematological diseases, respiratory diseases, muscle skeleton diseases, neurological diseases and urological diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of P2Y1 as well as pharmaceutical compositions comprising such compounds.
CN101274095A Humic acid detoxification peptide compound preparation and method for preparing the same The invention provides a compound preparation of humic acid and detoxification peptide, which comprises the following components: 0.1g of sodium humate or kalium humate, 0.1 to 1g of glutathione, 0 to 10g of cysteine, 0 to 10g of acetylcysteine, 0 to 10g of methionine and 0-10g of glycin. The compound preparation of the invention is used for relieving the toxicosis of fish, poultry and livestock, has good detoxification effect and high efficiency. The invention also provides a preparation method of the compound preparation of humic acid and detoxification peptide.
US20120040952 Azetidines as histamine h3 receptor antagonists The invention relates to compounds of formula (I), wherein R, R1, m, n and X1 to X3 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
CN103405610A Compact-type water-soluble human lubricant, preparation method of lubricant and condom The invention discloses a compact-type water-soluble human lubricant, a preparation method of the lubricant, and a condom using the lubricant. The compact-type water-soluble human lubricant comprises the following components in percentage by weight: 30-47% of glycerol, 2-4% of tween-20, 0.05-0.15% of sodium hyaluronate, 0.1-0.3% of jasminum essential oil, 0.5-1.2% of aloe essential oil, and 48-66% of water. The compact-type water-soluble human lubricant has good compatibility with the naturally-selected body fluid of human body, is not greasy, has a pH value as same as the pH value of the normal physiological environment of female vagina, and has the effects of nourishing vaginal tissues, promoting cell growth, increasing muscle elasticity, and improving vaginal relaxation.
US20090053299 Methods for generating immune response using cationic-liposome-mediated nucleic acid delivery The present invention is in the fields of drug delivery, and specifically, cationic liposome-based vaccines. In embodiments, this invention provides methods of making ligand-targeted (e.g., antibody- or antibody fragment-targeted) liposomes useful for the delivery of molecules to induce immune responses against viral antigens or to treat or prevent viral diseases. The specificity of the delivery system is derived from the targeting ligands.
US20120070475 Zero Calorie Polyphenol Aqueous Dispersions A method for stably dispersing microparticulated water insoluble bioactive polyphenol in a beverage by combining the bioactive polyphenol dissolved in an alkaline solution with an aqueous solution of at least one dispersion stabilizer. A composition comprising dispersed microparticulated water insoluble bioactive polyphenol(s) and a dispersion stabilizer.
EP2308847A1 Substituted pyridines as inhibitors of dipeptidyl peptidase IV and their application for the treatment of diabetes and related diseases The present invention relates to novel 2-aryl and 4-aryl substituted pyridines, which are highly selective and potent inhibitors of the dipeptidyl peptidase IV enzyme, and which are useful in the treatment and prevention of multiple diseases and disorders mediated by dipeptidyl peptidase IV, such as diabetes, particularly type II diabetes. The invention also relates to procedures for synthesis of such compounds and pharmaceutical compositions thereof. In view of the rapid increase of diabetes there is a considerable demand for the development of new agents in this field. There is particularly a need for agents with superior efficacy, high selectivity, long duration of action, better bioavailability, and physiological compatibility, which supplement the conventional therapies. The provided compounds are usable as really effective agents, exhibiting precious pharmacological properties as well as an excellent safety profile, for treatment and prophylaxis of diseases mediated by dipeptidyl peptidase IV, such as diabetes, particularly type II diabetes and related diseases.
EP2006300A2 Characterization of a calcium channel family Nucleic acids encoding SOC/CRAC calcium channel polypeptides, including fragments and biologically functional variants thereof and encoded polypeptides are provided. The nucleic acids and polypeptides disclosed herein are useful as therapeutic and diagnostic agents. Agents that selectively bind to the foregoing polypeptides and genes also are provided.
EP1495053B1 Angiopoietin-2 and angiopoietin-1 specific binding agents Disclosed are specific binding agents, such as fully human antibodies, that bind to angiopoietin-2. Also disclosed are heavy chain fragments, light chain fragments, and CDRs of the antibodies, as well as methods of making and using the antibodies.
US20110021517 Antitumor combination comprising a morpholinyl anthracycline derivative and demethylating agents The present invention provides a combination of a morpholinyl anthracycline derivative, in particular a methoxy morpholino doxorubicin derivative, or a pharmaceutically acceptable salt thereof, and a demethylating agent, having an antineo-plastic effect. Also provided is the use of the said combinations in the treatment or prevention of metastasis, in the treatment of tumors, as well for reversing the resistance in cells resistant to such a methoxy morpholino doxorubicin derivative.
CN102349935A Purpose of ginkgolic acid in preparing external preparation for treating venereal disease, gynopathy and perianal disease The invention relates to purpose of ginkgolic acid in preparing external preparations for treating venereal diseases, gynopathy and perianal diseases. The ginkgolic acid comprises ginkgolic acid, ginkgol, ginkgo dipenol, etc., and can be obtained from extractives of ginkgo leaf, fruit, episperm and rhizome through a chemical separation method. The venereal diseases comprise infectious and inflammatory genital diseases. A medicament, a disinfectant or external preparation containing ginkgolic acid for treating venereal diseases, gynopathy and perianal diseases comprises 0.001-80wt% of ginkgolic acid and a pharmaceutically common used external preparation matrix or a pharmaceutically accepted carrier, wherein the preparation is any pharmaceutical external dosage form. Pharmacological tests show that the preparation of the invention has substantial effects of killing resident pathogens on or surrounding genitals, resisting inflammation, relieving pain and itching. Clinic trials show that the preparation of the invention has outstanding curative effects on a plurality of venereal diseases, gynopathy and perianal diseases and an effective rate of 100%, and is safe for usage without side effect.
CN103462991A Application of Aphanamgrandiol A in preparation of anti-bacterial medicaments The invention relates to application of Aphanamgrandiol A in preparation of anti-bacterial medicaments, and belongs to the field of medicaments. Aphanamgrandiol A has a good effect on inhibiting Escherichia coli, pseudomonas fluorescens, staphylococcus aureus and proteus, and is expected to be applied to prepare the anti-bacterial medicaments. The application of Aphanamgrandiol A in the preparation of the anti-bacterial medicaments is disclosed for the first time, is impossibly prompted by any other compounds and has prominent substantive features, and meanwhile, Aphanamgrandiol A obviously has significant progress on preventing and treating bacterial infections.
CN1826118B Multiparticulates Multipartulates of oxycodone can be made by extrusion of a blend which suitably contains (a) oxycodone, (b) water-insoluble ammonium methacrylate copolymer, (c) plasticiser, (d) lubricant and (e) water permeability modifier.
WO2009110324A1 Method for regulation of expression of low-density lipoprotein receptor, and enhancer of expression of low-density lipoprotein receptor Disclosed are a novel method for regulating the expression of a low-density lipoprotein receptor (LDLR) and a novel enhancer of the expression of a LDLR, both of which can increase the expression level of a LDLR. The expression level of a LDLR can be increased by inhibiting the expression of a ZFP36 family. The inhibition of the expression of the ZFP36 family can utilize an expression vector which carries at least member selected from an antisense strand, double-stranded RNA and low-molecular-weight interfering RNA all for mRNA of the ZFP36 family or an expression vector which can express the at least one member.
US20100267806 LIPID FORMULATED COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION OF Eg5 AND VEGF GENES This invention relates to compositions containing double-stranded ribonucleic acid (dsRNA) in a lipid formulation, and methods of using the compositions to inhibit the expression of the Human kinesin family member 11 (Eg5) and Vascular Endothelial Growth Factor (VEGF), and methods of using the compositions to treat pathological processes mediated by Eg5 and VEGF expression, such as cancer.
CN102764249A Use of geranylgeranylacetone for preventing and treating renal injuries caused by morphine The invention relates to the novel use of geranylgeranylacetone for preventing and treating renal injuries caused by morphine. The geranylgeranylacetone can be used for protecting renal cells from the poison of the morphine, suppressing cell apoptosis caused by the morphine, weakening lipid peroxidation damage caused by the morphine, and preventing and treating the renal injuries caused by the morphine.
CN103360407A Thiophene miazines derivate as well as preparation method and medical application thereof The invention discloses thiophene miazines derivates as well as a preparation method and a medical application thereof. The thiophene miazines derivates are compounds with a general formula I, a general formula II or a general formula III, wherein in the general formulae, Ar is any one of phenyl, halogen-substituted phenyl, C1-6 alkyl-substituted phenyl, biphenylyl, halogen-substituted biphenylyl, naphthyl, pyridyl, thienyl, halogen-substituted thienyl, C1-3 alkyl-substituted thienyl, furyl, halogen-substituted furyl and C1-3 alkyl-substituted furyl, A, D and E are respectively carbon atoms or nitrogen atoms but are not carbon atoms at the same time, and R is R1-NH-. The thiophene miazines derivates provided by the invention can be used for obviously restraining the activity of an EGFR (Epidermal Growth Factor Receptor) and the activity of A431 cells, are expected to be developed as a tyrosine kinase inhibitor, and are extensive in application prospect and medicinal value.
WO2012158312A2 Skin and hair regeneration using polysaccharide-based hydrogels Methods for promoting skin regeneration, promoting hair follicle regeneration, and reducing scarring by topically administering polysaccharide-based hydrogel compositions to injured skin are presented.
WO2012011752A3 Novel long-acting glucagon conjugate and pharmaceutical composition comprising the same for the prevention and treatment of obesity Disclosed is a novel long-acting glucagon conjugate in which glucagon or its derivative is covalently linked to a polymer carrier via a non-peptide linker, and a pharmaceutical composition comprising the same as an effective ingredient useful for the prevention and treatment of obesity. Since the long-acting glucagon conjugate of the present invention shows improved in vivo durability and stability, when used in combination with an anti-obesity drug, it is possible to induce synergistic effects on the loss of body weight and decrease in food intake without causing any side-effects such as fluctuation in blood glucose level. Accordingly, the long-acting peptide conjugate of the present invention is very effective for the prevention and treatment of obesity.
US7510825 Detecting perturbations and alterations of the normal organization of the cell plasma membrane (PNOM)-cells within a population of cells using a "perturbed membrane-binding compound" (PMBC) of given formula; e.g. monitoring aggressiveness of a tumor The present invention provides kits and in vitro, in vivo or ex vivo detection methods by using compounds that bind selectively to cells undergoing perturbations and alterations of the normal organization of their cell membranes, such as cells undergoing apoptosis, while binding to a lesser degree to normal cells.
CN103356537A Application of Sarcaboside B in preparation of medicines for resisting aseptic inflammation The invention relates to an application of Sarcaboside B in the preparation of medicines for resisting aseptic inflammation. The inflammation refers to the aseptic inflammation. The Sarcaboside B has a good anti-inflammatory effect. The application of the Sarcaboside B in the preparation of the medicines for resisting aseptic inflammation is disclosed by the invention for the first time. As the skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpected strong inhibitory activity on inflammation, and the possibility that other compounds provide revelation does not exist. The Sarcaboside B has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for resisting inflammation.
CN102727772A Method for raising content uniformity of vitamin C in vitamin C forsythia granules A method for raising content uniformity of vitamin C in vitamin C forsythia granules is characterized in that prepared Lonicera and forsythia extract granules and coated vitamin C granules are respectively filled into two cups of a double-cup granule racking machine; and after one cup of the double-cup granule racking machine is filled with 9 g of the forsythia extract granules and the other cup is filled with 1 g of the coated vitamin C granules, the extract granules and the granules are respectively and simultaneously placed into a same packing bag, and the packing bag can be instantly sealed. By the utilization of the technology to prepare the vitamin C forsythia granules, a mixing step before split charging of the two kinds of granules is saved, and the two kinds of granules are directly placed into the same packing bag respectively through the double-cup granule racking machine. Mixing is finished in the bag such that it is ensured that the content of vitamin C in each bag of the vitamin C forsythia granules remains stable and the product vitamin C forsythia granules is completely qualified.
CN101057849A Slow-releasing preparation containing metformin hydrochloride and glipizide and its preparation method The invention discloses a diabecron and glipizide -containing slow-release agent and the method for preparing the same. The glipizide micro-pill takes blank micro-pill as carrier, and combines glipizide and other medical findings with it. The diabecron-containing slow-release micro-pill comprises diabetosan pill, slow-release coating membrane material or other medical findings. The method for preparing diabecron-containing slow-release micro-pill takes extrusion rolling method or blank micro-pill loading method. The product is characterized by safety, high efficient, low toxicity and convenient usage. It can be used to treat non-insulin-dependent diabetes mellitus.
CN103610702A Rheumatalgia ointment and preparation method thereof The invention discloses a rheumatalgia ointment, comprising the following raw materials in parts by weight: 20-60 parts of realgar, 50-160 parts of cantharides, 5-9 parts of Tibetan musk, 10-20 parts of borneol and 10-20 parts of dragon tail. The preparation method disclosed by the invention comprises the following steps: taking the raw materials; mixing and crushing the dragon tail and the Tibetan musk for dormancy at the temperature of about 0 DEG C for 24 hours for late use; independently crushing the realgar into fine powder which is about 500 meshes for late use; independently crushing the borneol into the fine powder which is about 500 meshes for late use; crushing the cantharides into fine powder which is about 500 meshes in a sealed machine for late use; mixing the fine powder in a sealed agitator, and precipitating well for an hour; taking proper amount of medicinal vaseline or propolis; melting at the temperature over 60 DEG C and cooling to about 15 DEG C, and then adding the evenly agitated fine powder to ferment for 48 hours. The rheumatalgia ointment has a significant curative effect on cold joint pain, typhoid fever pain and the like.
EP2671884A1 New 6,11-dihydro-5H-benzo[d]imidazo[1,2-a]azepines derivatives as histamine H4 receptor ligands The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.
CN102038707A Method for preventing and treating sow metritis The invention discloses a method for preventing and treating sow metritis. For a pig with metritis, the appetite is poor or lost, the body temperature is raised, the nose tray is dry, the pig frequently shows straining, and a large amount of yellow-white or brown smelly secretions flow out of the vagina and are frequently mixed with embryonic membrane debris. If the pig is not treated in time, sepsis or pyemia is often formed. The uterine mucous membrane can become thicken gradually due to chronic stimulation of inflammation, and the secretions periodically flow out of the vagina of a sick pig. Although the pig is estrous periodically, the pig is infertile after multiple times of mating. Chronic metritis is often accompanied by systemic symptoms. A hog house should be kept clean and dry, and clean bedding has to be replaced when a sow is parturient. During delivery assistance, strict attention should be paid to sterilization, and operations are required to be light and meticulous. After delivery, breeding management should be enhanced, and artificial fecundation should strictly follow a sterilization system. After taking all fetuses and embryonic membranes in dystocia, an antibiotic is filled into a capsule, and then the capsule with the antibiotic is directly slipped into the uterine cavity to prevent the metritis.
CN102482257A Apoptosis signal-regulating kinase inhibitors The present invention relates to compounds of Formula (I),wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase ("ASKl") inhibitory activity, and are thus useful in the treatment of ASKl -mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
US20110046129 2-Phenylethylamino Derivatives as Calcium and/or Sodium Channel Modulators 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.
CN1875931A An anticancer sustained release agent carrying angiogenesis inhibitor and cytotoxic drug Disclosed is an anticancer slow release injection carrying both anti-angiogenesis agent and cytotoxic drugs, which comprises slow release micro-balloons and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. the anti-angiogenesis agent is selected from Marimastat, SU5416, SU6688, Fumagillin and / or TNP-470, the cytotoxic drugs are selected from anti-taxone, alkylating agent, Topo enzyme inhibitor and/or plant alkaloid, The slow release auxiliary materials are selected from Polifeprosan, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid), ethylene-vinylacetate copolymer, the viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C).
WO2008037937A3 Use of compounds of the milbemycin family for the treatment of dermatological disorders in human beings The present invention relates to the use of compounds of the milbemycin family or derivatives thereof for producing a pharmaceutical composition for the treatment of dermatological affections in human beings, in particular rosacea.
WO2013151877A1 Pyrimidinedione carboxamide inhibitors of endothelial lipase The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
CN101163677B Crystalline forms of a biphenyl compound The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystallinecompounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
CN102106900A Formula of compound lamiophlomis-root dripping pill The invention discloses a formula of a compound lamiophlomis-root dripping pill. The dripping pill mainly comprises lamiophlomis-root extract and borneol as main components, and is prepared from the lamiophlomis-root extract, the borneol and appropriate matrixes in certain proportions. Compared with other dosage forms, the dripping pill preparation has the advantages of short process flow, low production cost, quick effect response, good analgesic effect, unique formula and manufacturing method, and remarkable therapeutic effect.
CN1879860A Natural herbal hair tonic The invention discloses a hair tonic agent which is prepared from natural plants including arborvitae tops, wolferry fruit, dried ginger, arborviate seed, drynaria, root of red rooted saliva, Siberian solomonseal rhizome, clove, ligustrum japonicum, boneol, menthol, geranium, safflower, dried rehmannia root, radix paeoniae rubrathe and peach kernel.
US20120322813 Rutaecarpine derivatives for treating caffeine toxicity The teachings provided herein generally relate to compositions comprising a rutaecarpine derivative that activates CYP1A2 through enzyme induction. The compound can be used for treating caffeine toxicity, in some embodiments. Caffeine is just one example of a substrate that can be removed using the derivatives taught herein, and other examples, including theophylline, are provided herein.
EP1530565A1 Substituted thiophene carboxamide compounds for the treatment of inflammation The present invention provides substituted thiophene carboxamide compounds having structural Formula I and isomers, tautomers, polymorphs, carriers, prodrugs, and pharmaceutically acceptable salts thereof, compositions comprising such, and methods for treating diseases associated with kinase activity. More specifically, the present invention provides methods of treatment of a variety of diseases associated with IKK2 including the treatment of inflammation, other inflammation-associated disorders, such as, as an analgesic in the treatment of pain and headaches, arthritis, including but not limited to rheumatoid arthritis, asthma, gastrointestinal conditions such as inflammatory bowel disease, vascular diseases, viral infections such as AIDS, and cancer.
WO2005113534A3 Cxcr1 and cxcr2 chemokine antagonists The present invention is directed to a compound having the general structure of formula (1) useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.
CN101524447A Pharmaceutical composition for treating constipation and preparation process thereof The invention discloses a pharmaceutical composition for treating constipation and a preparation process thereof. The pharmaceutical composition is prepared by taking senna leaf, hemp fruit, black sesame, natrii sulfas exsiccatus, white paeony root, flower of Japanese pagodatree, mulberry leaf, trifoliate akebia, herba schizonepetae, and oriental waterplantain rhizome in proportion by weight, and can be prepared into any common preparation for oral administration which comprises granules, capsules, pills, tablets, and the like. The medicament of the invention can effectively treat the constipation, can relieve abdominal pain and bloating caused by the constipation, ensures that symptoms of the constipation are disappeared, and has the advantages of short treatment course, quick response, and no side effects; moreover, the recurrence of the constipation cannot be caused by stopping taking the medicament, and the medicament is a preferred effective medicament for treating the constipation; and the medicament has obvious curative effects on blood deficiency and intestinal dry, relaxing bowel, abdominal fullness and distention, and promotion of excretion.
US20110159057 Hydroxyapatite and bioglass-based pellets, production process and applications of thereof The disclosed subject matter refers to hydroxyapatite and bioglass-based pellets of homogeneous size and spherical shape, whose interconnective porous structure, in the micrometer range, allows for an enhanced osteoconductivity and osteointegration, with specific application as a synthetic bone graft and to the respective production process. The production process is based on the pharmaceutical technology of extrusion and spheronization employing a porogenic agent and applying a sinterization stage in the presence of a vitreous liquid phase, which reverts on behalf of a higher reproducibility, superior yield and greater production capacity. Therefore, the disclosed subject matter is directed to the production of hydroxyapatite and bioglass-based pellets with applications in osteoregenerative medicine, particularly in the fields of orthopaedic surgery, maxillofacial surgery, dental surgery, implantology and as tissue engineering scaffolds
US20050020671 Core comprises first active ingredient, coating comprising second active ingredient incompatible with first and barrier between core and coating which prevents physical contact between them, characterised in that barrier is formed on core by film-coating and coating is formed by press-coating The present invention provides a pharmaceutical formulation which comprises a core comprising a first active ingredient, a coating comprising a second active ingredient which is incompatible with the first active ingredient and a barrier between the core and the coating which prevents physical contact between the core and the coating, characterised in that the barrier is formed on the core by film-coating and the coating is formed on the barrier by press-coating.
CN102731510A Derivatives of ticagerlor, and preparation method and pharmaceutical application thereof The invention provides derivatives of ticagerlor or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 in a formula representing the derivatives or the pharmaceutically acceptable salts thereof can be selected from amino acid residues or acetylsalicyloyl groups. The invention also provides a preparation method for the derivatives of ticagerlor or the pharmaceutically acceptable salts thereof and further provides application of the derivatives of ticagerlor or the pharmaceutically acceptable salts thereof in preparation of drugs used for treating blood coagulation-related diseases. The derivatives provided in the invention can improve bioavailability of ticagerlor or enhance the drug combination effect of ticagerlor and aspirin.
US20120282290 Mycobacterial Vaccines There is provided a fusion protein or a polynucleotide sequence encoding said fusion protein that comprises first and second domains, wherein the first domain of the fusion protein comprises an amino acid sequence having at least 70% sequence identity to the amino acid sequence of SEQ ID NO: 1, or a fragment thereof comprising at least 20 consecutive amino acids thereof; and wherein the second domain of the fusion protein comprises a mycobacterial antigen or an antigenic fragment thereof. Also provided are corresponding therapeutic uses thereof for the protection of primates against mycobacterial infections.
WO2008080937A1 2-substituted pyrimidines i in therapy The present invention relates tothe use of 2-substituted pyrimidines of the formulaI (I) or the pharmaceutically acceptable salts thereof in therapy. In formula Ithe indices and the substituents are as definedin the claims and the specification.
CN103382206A Quinoline or quinazoline derivative, its preparation method and application in medicines The invention relates to a quinoline or quinazoline derivative, its preparation method and an application in medicines, specifically to new quinoline or quinazoline derivative as shown in a general formula (I) and its medicinal salt or a pharmaceutical composition containing the derivative and a preparation method thereof. The invention further relates to an application of the quinoline or quinazoline derivative and its medicinal salt or the pharmaceutical composition containing the derivative in the preparation of a therapeutic agent, especially a protein kinase inhibitor. Each substituent group in the general formula (I) has the same definition as in the specification.
CN102614164A Application of salvianolic acid A in pharmacy The invention discloses application of salvianolic acid A in pharmacy, and relates to application of salvianolic acid A in terms of preparation of medicines for suppressing activation of renal fibroblasts and intercapillary cells, preparation of medicines for reducing renal fibrosis, preparation of medicines for improving urine protein, preparation of medicines for improving renal functions, preparation of medicines for relieving renal inflammation and collagen deposition and preparation of medicines for relieving related genes and protein of renal fibrosis indexes. A screening platform for activation of renal fibroblasts and intercapillary cells of mice induced by TGF (transforming growth factor)-beta 1 is designed, and experiments show that from 4.94X10-5g/ml to 4.94X10-5g/ml of salvianolic acid A can suppress activation of the renal fibroblasts and intercapillary cells of the mice induced by the TGF-beta 1. A vitro experiment of the salvianolic acid A functioning to the mice in a UUO (unilateral ureteral obstruction) model and a Platt model is further designed and shows that medium-dosage salvianolic acid A (10mg/kg/d) and high-dosage salvianolic acid A (17.1mg/kg/d) can reduce urine protein, renal functions and related genes and protein of renal fibrosis of the mice in the UUO model and the Platt model.
CN102134243A Bicyclic amino pyrazole derivatives with anti-tumor activity The invention relates to bicyclic amino pyrazole derivatives and an application thereof in treatment of tumors, research results show that compounds have a role in significantly inhibiting tumor cells, wherein a plurality of compounds are obviously better than a positive control medicament, namely Rescovitine, on the cell level, and the bicyclic amino pyrazole derivatives are expected to be studied and developed into clinically effective anti-tumor medicaments.
US20090291134 Endoxifen methods and compositions in the treatment of psychiatric and neurodegenerative diseases The present invention provides compositions containing endoxifen, formulations and liposomes of endoxifen, methods of preparation of such agents and formulations, and use of such agents and formulations for the treatment of a subject having or at risk for psychiatric and neurodegenerative diseases. Specifically, the present invention relates to the composition comprising endoxifen in the treatment of bipolar disorder, schizophrenia, multiple sclerosis (MS), Alzheimer disease, Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis (ALS), and/or epilepsy by administrating formulations or compositions comprising an effective amount of endoxifen.
CN103599095A Application of Hippolachnin A in drugs for treatment and prevention of renal fibrosis Belonging to the technical field of new application of drugs, the invention discloses application of Hippolachnin A in drugs for treatment or prevention of renal fibrosis for the first time. Hippolachnin A has a brand new skeleton type, strong renal fibrosis inhibitory activity, and prominent substantive features. At the same time, application of Hippolachnin A in prevention and treatment of renal fibrosis obviously has significant progress.
EP1809298A2 Neuroprotective spirostenol pharmaceutical compositions The present invention relates to methods, kits, combinations, and compositions for treating, preventing or reducing the risk of developing a disorder or disease related to, or the symptoms associated with a neurodegenerative disorder such as neurotoxicity or a neuropathology in a subject, particularly to beta-amyloid-induced neurotoxicity and Alzheimer's disease. The invention further provides a method for inducing stem cell differentiation into neuronal cells, by administering to the patient a therapeutically effective amount of a compound of the invention.
WO2011074903A3 Pharmaceutical composition containing a3 adenosine receptor agonist The present invention relates to a pharmaceutical composition for prevention and treatment of inflammatory diseases, colon cancer and prostate cancer, the composition including selective A3 adenosine receptor agonist, 2-chloro-N6-(3-iodobenzil)-4'-thioidenosine-5'-N-methyluronamide (thio-Cl-IB-MECA), N6-(3-iodobenzil)-4'-thioidenosine-5'-N-methyluronamide (thio-IB-MECA), or pharmaceutically acceptable salts thereof. The pharmaceutical composition according to the present invention is useful for prevention and treatment of inflammatory diseases because of the remarkably lower toxicity thereof compared with typical A3 adenosine receptor agonists. In addition, the pharmaceutical composition according to the present invention is useful for prevention and treatment of colon cancer and prostate cancer because of the more selective inhibition thereof against growth of androgen receptor-dependent or non-dependent prostate cancer cells compared with typical A3 adenosine receptor agonists.
EP1975159A1 2,3,4,9-Tetrahydro-1H-carbazoles The present invention relates to 2,3,4,9-tetrahydro-1 H-carbazoles of the general formula I, in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
CN101279970A 2-methyl-5-azomycin-1-(3-chloro-2-hydroxypropyl) chloro-substitutied derivate, preparation and application thereof The invention relates to a compound with general formula(I), and pharmaceutically acceptable salt and hydrate thereof. Compared with prior art, the compound has the following advantages: the compound is of better curative effect in antisepsis, better trichomonacidal activity and less side effects.
US7428705 Web map tool A method of mapping at least a part of one or more web sites having web objects and web links is provided, whereby web objects and links are mapped as nodes and edges, respectively, in one or more web maps, each object being mapped to at least one corresponding node. The method allows a user to re-display selected items in a web map such that the item are distinguished from other items in the web map and are displayed in a clarified form. This enables a web map to be de-cluttered.
US20090298800 1,25-dihydroxy, 20-cyclopropyl,26-27-deuteroalkyl vitamin d3 compounds and methods of use thereof The invention provides vitamin D3 analogs of cholecalciferol, substituted at carbons-26 and 27 with deuterated alkyl groups, e.g., trideuteromethyl, wherein carbon-16 is a single or double bond, and carbon-23 is a single, double, or triple bond. The invention provides pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.
US20090048249 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders The present invention is directed to novel 3-benzoimidazolyl-pyrazolopyridine compounds of formula (I): and pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of serine-threonine protein kinases and tyrosine protein kinases and interactions thereof.
EP1675823B1 Phenethanolamine derivatives for the treatment of respiratory diseases Compounds of formula (I), and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective β2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).
CN102178833A Medicine for treating toothache The invention discloses a medicine for treating toothache. The medicine is prepared by the step of: decocting 18g of angelica sinensis, 18g of radix rehmanniae, 21g of Chinese coptis root, 15g of radix scutellariae, 12g of radix ophiopogonis, 30g of gypsum, 15g of cortex moutan, 6g of wild ginger, 12g of prepared rhizome of rehmannia, 12g of platycodon root, 18g of liquorice, 18g of rhizoma corydalis and 1500ml of water to be 250ml; and the medicine for treating toothache is taken in the morning and night on an empty stomach. The medicine for treating toothache disclosed by the invention has the curative effects of clearing away heat and toxic materials, and cooling blood and activating the blood circulation, and has fast and excellent curative effect when applied to treating the toothache; in addition, the total efficiency is up to 96.5%.
WO2014138920A1 Method for extracting organic solids and oil from marine organisms enriched with astaxanthin The present invention relates to a method for extracting shrimp oil. Particularly, shrimp processing water (EPC) is recovered and subjected to a dissolved air flotation (DAF) system after adding a flocculating agent. The suspended and dissolved solids form aggregates that are recovered from the surface by means of a procedure referred to as "skimming". The skimming product is then directed into a horizontal centrifuge (settling tank) in order to separate the solid phase (SOC) and the liquid phase consisting of water and shrimp oil. The liquid phase is pumped into the 3-phase vertical centrifuge in order to separate the shrimp oil, the water, and the solids. The solids recovered after using the separator can then be added to the solid phase obtained after settling. The resulting shrimp oil is very rich in astaxanthin, and the resulting water contains very little organic material and can be returned to the general processing plant effluent.
US20070293538 Pharmaceutical Composition And Methods For Treating Neurodegenerative Disorders The invention provides compositions and methods for treating neurodegenerative disorders. The method of the invention involves administering to an individual in need of treatment a composition having an R-NSAID or a derivative thereof and a SSRI. The methods and compositions of the invention are useful for treating and preventing neurodegenerative disorders such as Alzheimer's disease, dementia, and mild cognitive impairment.
CN103705485A Composite for treating myelodysplastic syndrome and preparation method thereof The invention discloses a composite for treating myelodysplastic syndrome. The composite comprises the following components: lenalidomide, a carrier, a solubilizing agent, a disintegrating agent, a lubricating agent, a flow aid and an adhesive, wherein the carrier is a mixture of any one or several of a high-molecular water-soluble polymer, a water-soluble small molecule compound, a hydrophilic auxiliary material and an inorganic carrier; the solubilizing agent is a mixture of one or several of lauryl sodium sulfate, poloxamer, beta. cyclodextrin and a derivative thereof, polysorbate and polyoxyethylene alkyl ether. The invention also provides a preparation method of the composite, and the preparation method comprises the steps of grinding, mixing, dry granulation, total mixing and tabletting or capsule filling. The preparation method disclosed by the invention effectively enhances the water solubility and bioavailability of the lenalidomide; the dry granulation preparation process simplifies the preparation steps, reduces the cost, saves the energy resources, reduces the labor expenditure and realizes the energy conservation and environment protection in production.
WO2010079221A1 Pharmaceutical composition comprising one or more fumaric acid esters A pharmaceutical controlled release composition comprising one or more fumaric acid esters.
US7271198 Administering to a patient suffering from autoimmune disease a treatment effective amount of a histone hyperacetylating agent, or a salt A method of treating an autoimmune disease comprising administering to the subject a treatment effective amount of a histone hyperacetylating agent, or a pharmaceutically acceptable salt thereof.
US20080069772 Treatment of transformed or infected biological cells The present invention relates to a therapeutic or/and diagnostic substance. Furthermore it relates to an expression vector, to a composition comprising the afore-mentioned substance or/and the afore-mentioned expression vector, a method for diagnosing a tumor disease or/and an infectious disease in a living being, as well as to a method for the treatment of a tumor disease or/and of an infection in a living being.
US20120164216 Pharmaceutical composition of duloxetine or pharmaceutically The invention relates to a taste masked pharmaceutical composition comprising duloxetine or pharmaceutically acceptable salts thereof. The invention also relates to processes for the preparation of such compositions. The invention further discloses an inclusion complex comprising duloxetine or pharmaceutically acceptable salts thereof with one or more cyclodextrin or derivatives thereof.
CA2669104A1 Hydrindane analogs having sphingosine 1-phosphate receptor agonist activity Hydrindane analogs of formula (IA) and (IB) that have agonist activity at one or more of the SlP receptors are provided. The ' compounds are sphingosine analogs, which, after phosphorylation, can behave as agonists at SlP receptors.
CN101428021B Externally used medicament preparation for quitting tobacco and wine The invention relates to an external medicine preparation used for abstaining from craving for tobacco and wine. The external medicine preparation is characterized in that the active ingredient for preparing the medicine is cytisine and/or the pharmaceutically acceptable salt thereof. The external medicine preparation comprises the following active ingredients by the weight percentages: 0.001% to20% of cytisine or the pharmaceutically acceptable salt thereof and auxiliary materials in balancing amount. The external used medicine can be produced into any pharmaceutically acceptable external dosage form, and has strong practicability when being used for abstaining from craving for tobacco and wine.
US20080287394 hydroxy-substituted pyrazinopyrrolopyridazine dione compounds; viricide; infection by HIV, AIDS; with other HIV/AIDS antivirals, immunomodulators, antibiotics or vaccines; 2-(2-fluorobenzyl)-10-hydroxy-4,8-dimethyl-7,8-dihydropyrazino[1',2':1,5]-pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-dione Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
US6919072 Comprises matrix metalloproteinase (MMP) inhibitor; for promoting collagen production Chronological aging of human skin can be delayed with the topical application of an MMP inhibitor, preferably a retinoid (an indirect MMP inhbitor); retinoids also normalize procollagen biosynthesis. Chronological aging, or natural aging, is evidenced in elderly (80+ years old) skin by increased MMP levels and decreased procollagen levels when compared with younger individuals. Prophylactic treatment of not yet chronologically-aged skin with a retinoid both inhibits degradation of dermal collagen and restores procollagen synthesis. Biopsied sections from elderly skin show that a single treatment of chronologically-aged skin with a retinoid can increase epidermal thickness, improve the dermal collagen density, and promote the formation of rete pegs and dermal papillae. Such benefits are helpful in preventing bruising, tearing, and ulceration of elderly skin. Accordingly, prophylactic treatment begun much earlier in life with an MMP inhibitor and/or a retinoid delays the onset of such symptoms.
EP1854880A1 Methods and reagents for modulating cholesterol levels The invention features ABC1 nucleic acids and polypeptides for the diagnosis and treatment of abnormal cholesterol regulation. The invention also features methods for identifying compounds for modulating cholesterol levels in an animal (e.g., a human).
CN102007106A 3-substituted-1,4-diazepan-2-one melanocortin-5 receptor antagonists The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases. Formula (I).
EP1233943B1 Ionizable indolinone derivatives and their use as ptk ligands The present invention features formulations of indolinones which compounds are ionizable as free acids or free bases. The formulation is suitable for parenteral or oral administration, wherein the formulation comprises an ionizable substituted indolinone, and a pharmaceutically acceptable carrier therefor. The term 'ionizable substituted indolinone' includes pyrrole substituted 2-indolinones which, in addition to being otherwise optionally substituted on both the pyrrole and 2-indolinone portions of the compound, are necessarily substituted on the pyrrole moiety with one or more hydrocarbon chains which themselves are substituted with at least one polar group. The formulations and the compounds themselves are useful for the treatment of protein kinase related disorders as discussed herein.
CN101306010A Function food for reducing the blood sugar and preventing diabetes complicating disease The invention discloses a functional food used for reducing blood sugar and preventing diabetes mellitus complications, which comprises the active ingredients by the weight percentages as follows: 10 to 70 percent of alginate, 15 to 75 percent of taurine, 10 to 70 percent of L-arginine and 0.01 to 5 percent of nutrient chromium. In the active ingredients of the functional food, the alginate has the function of improving the glucose tolerance, the nutrient chromium is the nutrients for a patient, the taurine has the antioxidation function, and the L-arginine has the function of improving the blood vessels. The functional food combines the functions of the alginate, the taurine, the L-arginine, and the nutrient chromium according to a certain rule, and manufactures the functional food according to a certain component proportion, thereby leading the alginate, the taurine, the L-arginine, and the nutrient chromium to be put into full-play during the process of reducing blood sugar and preventing diabetes mellitus complications.
CN1927271A Receptor smoking giving up plaster The invention relates to an acceptor no-smoking plaster, which comprises mint, clove, liquorice, tobacco, vitamin E, vitamin B5, release-control agent, skin penetrate agent, pressure-sensitive adhesive, and innocuous derivative Valine-C1 in nicotine group which can replace the nicotine. Wherein, the production comprises that mixing the extractives of mint, clove, liquorice, and tobacco with vitamin E, vitamin B5 and Valine-C1, adding release-control agent, skin penetrate agent and pressure-sensitive adhesive, to be mixed uniformly; then coating, drying and cutting into final product. The invention uses Valine-C1 to replace nicotine, and uses tobacco extractive to replace nicotine to directly function the acceptor, to reduce the cost and the toxicity.
US20080188520 e.g. 1-(2-Cyclopropylmethoxy-1,2-diphenylethyl)-1H-pyridin-2-one; potassium (K+) channel-blocking agent; potassium channel KACh and TASK-1 channel blocking agent; atrial arrhythmias, atrial fibrillation or atrial flutter; respiratory disorders, neurodegenerative disorders; anticarcinogenic agent The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
WO2010040212A1 Processes for the preparation of erlotinib hydrochloride There is provided processes to prepare erlotinib hydrochloride. The processes may comprise exposing solid erlotinib free base containing residual solvent to hydrogen chloride gas. The processes may comprise spraying hydrogen chloride gas in an organic solvent onto solid erlotinib free base. Erlotinib hydrochloride prepared by such methods is also provided.
CA2661503A1 Inhibitors of 11.beta. -hydroxysteroid dehydrogenase type 1 This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11.beta.- HSDl in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
US20120058185 Stable pharmaceutical compositions of olanzapine and process for their preparation The present invention provides a stable pharmaceutical composition of Olanzapine or its pharmaceutically acceptable salt comprising coated tablet formulations of Olanzapine or its pharmaceutically acceptable salt, wherein the coating consists essentially of pectin or copovidone, and a process of making the same.
US20110046134 NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
US20110071163 Use of an opioid receptor antagonist for the treatment or prevention of gastrointestinal tract disorders The disclosure relates to a method of treating or preventing a condition in a subject associated with the activation of an opioid receptor in the periphery by administering an effective amount of 5-(2-methoxy-4-{[2-(tetrahydro-pyran-4-yl)-ethylamino]-methyl}-phenoxy)-pyrazine-2-carboxamide (Compound I). In particular, the disclosure relates to a method of treating or preventing opioid-induced constipation or opioid-induced bowel dysfunction in a human without reducing centrally-mediated opioid analgesia or producing central opioid withdrawal symptoms by administering an effective amount of Compound I. The disclosure further relates to the use of Compound I for the preparation of a medicament for the treatment or prevention of a condition in a subject associated with the activation of an opioid receptor in the periphery.
EP1736161A2 Use of an arsenic compound for the manufacture of a medicament for the treatment of arsenic susceptible blast-like cell related diseases Use of an arsenic compound for the manufacture of a medicament for treatment of arsenic-susceptible blast-like cell related diseases, such as hypersusceptible diseases, immune or autoimmune diseases, fibroblast-related diseases, inflammation diseases or parasitic diseases.
CN102161658A N-(naphthoxyalkyl)heteroarylpiperidine compounds and preparation method and applications thereof The invention relates to the pharmaceutical synthesis field and discloses N-(naphthoxyalkyl)heteroarylpiperidine compounds and a preparation method and applications thereof. The compounds disclosed by the invention are the compound shown in the formula I and pharmaceutically acceptable acid addition salts thereof, wherein n is 0, 1, 2 or 3; R is acetamino, acetoxy, acethythio, oximido, amino, aminocarbonyl, dimethylamino, diethylamino, hydroxyl, trifluoromethyl, trifluoroacetyl, cyano, phenyl, aldehyde group, benzoyl, fluorine, chlorine, bromine or iodine. The preparation method is as follows: 7-methoxynaphthalene compound used as raw material and 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole are used to perform N-alkylation reaction. The N-(naphthoxyalkyl)heteroarylpiperidine compounds can act on 5-HT2A receptor, dopamine D2 receptor and melatonin receptor, are the compounds with the multi-target function and have the antipsychotic function.
CN102786509A 2-(5,6-methylxanthone-4-yl)-acetic acid derivatives, preparation method and uses thereof The present invention provides a class of 2-(5,6-methylxanthone-4-yl)-acetic acid derivatives with a novel structure, wherein a structure of a general formula is represented by a picture. The present invention further provides a method for preparing the derivatives, wherein multiple structure modification reforming are performed on a carboxyl portion of 2-(5,6-methylxanthone-4-yl)-acetic acid to prepare the derivatives. Compared with the existing 2-(5,6-methylxanthone-4-yl)-acetic acid or derivatives thereof, a part of the derivatives prepared by using the method of the present invention provide inhibition effects for a variety of tumor cells, particularly provide high tumor cell inhibition rate for lung cancer and leukemia, and show significant anti-tumor activities. According to the present invention, the design is rational, sources of the raw materials for preparation are wide, the raw materials are easy to obtain, the preparation method is simple and easy to operate, reaction conditions are mild, the product yield is high, and the method is applicable for industrial large scale production.
EP0574579B1 Dna encoding a human 5-ht 1f receptor and uses thereof This invention provides an isolated nucleic acid molecule encoding a human 5-HT1F receptor, an isolated protein which is a human 5-HT1F receptor, vectors comprising an isolated nucleic acid molecule encoding a human 5-HT1F receptors, mammalian cells comprising such vectors, antibodies directed to the human 5-HT1F receptor, nucleic acid probes useful for detecting nucleic acid encoding human 5-HT1F receptors, antisense oligonucleotides complementary to any sequences of a nucleic acid molecule which encodes a human 5-HT1F receptor, pharmaceutical compounds related to human 5-HT1F receptors, and nonhuman transgenic animals which express DNA a normal or a mutant human 5-HT1F receptor. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and treatment involving the human 5-HT1F receptor.
CN103211827A Compound amoxicillin oil suspension prescription and preparation method thereof The invention relates to the technical field of a veterinary medicine preparation, and particularly relates to a veterinary medicine prescription and a new production process technology. The veterinary medicine prescription and the new technique of production process overcome the shortcomings of easy degradation of amoxicillin, short half-life period, wide antibacterial spectrum and the like. The new prescription and the preparation technology have the advantages that the medicine is non-degradable, long in half-life period, long-acting and controlled-release, and has wide antibacterial spectrum, synergistic interaction and the like. The compound amoxicillin oil suspension prescription is suitable for part of drug-resistant strain infection and mixed infection diseases.
EP1263435B1 Pharmaceutical composition for treatment and prevention of liver fibrosis and cirrhosis The present invention provides a pharmaceutical composition for treatment and prevention of liver fibrosis and cirrhosis, which comprises 5-(2-pyrazinyl)-4-methyl-1,2-dithiol-3-thione (oltipraz) and dimethyl-4,4"-dimethoxy-5,6,5",6"-dimethylene dioxybiphenyl-2,2"-dicarboxylate (DDB) as major components. The ratio of oltipraz and DDB of said composition is preferably 25:0-25, more preferably 5:0.1-5, particularly preferably 5:1. Oltipraz/DDB formulations according to the present invention exhibit surprisingly good effect on the treatment and prevention of liver fibrosis and cirrhosis and are safe drugs that have low toxicity in the human body.
CN103494828A Preparation method of sulfanilamide salt and trimethoprim soluble powder The invention relates to a preparation method of sulfanilamide salt and trimethoprim soluble powder. The preparation method is characterized in that after sulfanilamide salt and trimethoprim are treated through a special technology, the sulfamido alkaline drug and the trimethoprim acid medicine can simultaneously and uniformly disperse in water and do not precipitate within two hours, and the active ingredient content of the sulfanilamide salt and trimethoprim soluble powder is stable. The sulfanilamide salt and trimethoprim soluble powder is convenient to use for animals, has a definite curative effect and good stability and is safe and reliable without adverse reaction; and compared with a premix, the sulfanilamide salt and trimethoprim soluble powder has obvious clinical application advantage.
US20070293441 High-pressure sterilization to terminally sterilize pharmaceutical preparations and medical products The present disclosure provides a sterilized medical system that includes an ultra high pressure sterilized glucose solution in a container. The sterile glucose solution may contain less than about 40 ppm total glucose degradation product. The glucose solution may be a ready-to-use infusion solution disposed in a single chamber container.
EP2056817A1 Benzofuran and benzothiophene derivatives useful in the treatment of cancers of the central nervous system The present invention relates to benzofuran and benzothiophene derivatives and compositions containing such compounds for the production of medicaments for the treatment of cancers of the central nervous system as monotherapy or combination with other agents.
WO2010100297A1 Bisthiazole compounds that can be used to treat cancer The invention relates to compounds having formula (I), the pharmaceutically acceptable salts thereof, or the solvates of same, wherein: Ri is selected from phenyl, optionally mono-, di- or tri-substituted with a radical independently selected from F, Cl, Br, I, (C1C4)-alkyl, N,N-(C1,C4)-alkylamino, hydroxy, (C1C4)-alkoxy, phenoxy, methylenedioxy, trifluoromethoxy, trifluoromethyl, carboxyl, 4-phenoxyphenyl and (C1C4)-alkoxycarbonyl; 2-thiazolyl; 2-pyridinyl; 2,2'-bipyridinyl; 2,2'-bisthiazole; naphthyl; 4-phenoxyphenyl and isoquinolyl; R2 is selected from the same group as R1 and, in addition, is independent of H and I; and R3 and R4 are selected independently from H, Br and F. Said compounds inhibit cell proliferation of tumour cells independently of the p53 protein and can likewise induce apoptosis in different tumour cells independently of the p53 protein, making same suitable for use in the treatment of different types of cancer. Formula (I)
US8148429 Use of benzylideneaminoguanidines and hydroxyguanidines as melanocortin receptor ligands The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof.
US7560443 Mixtures of fructose, sucrose and lactose as a low-calorie bulk sweetener with reduced glycemic index Mixtures of fructose and lactose are useful for reducing caloric intake and glycemic index for individuals who are overweight, glucose-impaired, diabetic, or who just consume too large a fraction of their calories from “added sugars”. The fructose/lactose sweetener is included in the daily diet as a one-for-one replacement for “added sugars” in various edible formulations without sacrificing quality of taste. Sucrose can be used as a replacement for all or part of the fructose in the claimed sweetener to increase sweetness or improve certain functional properties without substantially changing caloric value. The claimed mixtures of fully-caloric sugars work synergistically to reduce available calories and blood sugar concentration. Specifically, fructose interferes strongly with normal small-intestinal absorption of lactose and interferes moderately with sucrose absorption, while lactose interferes with normal small-intestinal absorption of both sucrose and starch. Unabsorbed di- and oligosaccharides pass into the colon and cause increased growth of healthful bacteria, making the new sweetener useful as a prebiotic. No gastrointestinal symptoms of sugar intolerance were observed when the claimed sugar mixtures were ingested at normal dietary levels.
WO2011090316A3 Novel pyrazinone derivatives having an apoptosis-inducing activity, and pharmaceutical compositions comprising same The present invention relates to compounds selected from a group consisting of novel pyrazinone derivatives having an apoptosis-inducing activity, the pharmaceutically acceptable salts thereof, the isomers thereof, and the hydrates and solvates thereof, and to pharmaceutical compositions comprising the compounds as active ingredients. The compounds and the pharmaceutical compositions of the present invention can effectively treat diseases caused by the inhibition of apoptosis.
US20110237616 Phehylephrine formulations with improveds stability A pharmaceutical composition includes a pharmaceutical polysaccharide and phenylephrine hydrochloride. The ratio of said polysaccharide to phenylephrine hydrochloride is sufficient to dilute the composition such that phenylephrine hydrochloride is stable at high temperature and humidity.
EP2729141A1 Cyclic amine derivatives as ep4 receptor agonists There is described a group of novel cyclic amine derivative compounds having an EP4 receptor agonistic activity. Specifically, the compounds according to the invention are provided with analgesic, antiinflammatory, antiglaucoma activity, and also with anti-osteoporosis and antiulcerative activity. The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.
CA2178458C Stable complexes of crosslinked polyvinylpyrrolidone and iodine and method of making the same A wound treatment material which absorbs wound fluid without overdrying the wound, provides physical cushioning for the wound, and releases an antimicrobial agent (iodine) in a controlled manner to kill harmful micro--organisms without irritating the wound area or adversely affecting would healing. The wound treatment material comprises crosslinked polyvinylpyrrolidone-iodine complex which is water insoluble, but water-absorbent and water--swellable. When the complex or a wound treatment preparation containing the complex is applied to a wound, i.e., becomes hydrated, and an equilibrium is established between the complex and the wound at the wound/complex interface. Iodine is releaed from the crosslinked polyvinylpyrrolidone-iodine complex by a diffusion controlled process which responds to the reduction in concentration of free iodine in the wound fluid in equilibrium with the complex. The greater the rate of iodine depletion in the wound, the greater the rate of iodine release from the polymer-iodine complex. It has been discovered that this diffusion controlled release mechanism can be utilized to deliver antimicrobially effective amounts of iodine to the wound while maintaining the concentration of iodine below the concentration that could cause significant wound irritation or retardation of healing. It has also been found that the moist environment at the wound/complex interface and the physical protective effect (cushioning) offered by the hydrated complex can enhance wound healing.
US20120258099 Inhibitors of guanine exchange factors and their use as anticancer drugs A peptide including the amino acids sequence X9 CGYX13X14 AX16X17X18 MX20X21X22X23X24X25X26X27 CPLCX32X33, a nucleic acid coding for the peptide, and/or a recombinant vector including the nucleic acid for the preparation of a drug intended for the treatment of cancer.
WO2013047055A1 Heat shock protein expression inducer Provided is a heat shock protein expression inducer based on a heat shock protein (HSP) expression-inducing action. The present invention is a heat shock protein (HSP) expression inducer comprising eupalinolide A and/or B, the heat shock protein expression inducer being obtained by extracting eupalinolide A and/or B from the dried aerial part of the herb Eupatorium lindleyanum, and is also a method for extracting eupalinolide A and/or B, the method comprising fractionating an ethanol extract obtained by the ethanol extraction of Eupatorium lindleyanum, the fractionation being performed by a variety of column chromatography and HPLC techniques.
WO2014141132A1 NEW HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND β-LACTAMASE INHIBITORS The present invention relates to new heterocyclic compounds, their preparation and their use as β−lactamase inhibitors in combination with one or more antibiotics for the treatment of infections caused by β−lactamase-producing pathogenic bacteria.
EP2226078A2 Anti-fungual compounds and compositions The invention relates to compounds and compositions with antifungal activity, particularly against onychomycosis. Particularly, the invention is directed to use of fermented cereal grain for treatment of fungal infections, to composition with Lactobacillus species fermented cereal grain and a penetration enhancer, to an applicator comprising a brush, a reservoir, a cap, and a liquid composition comprising fermented cereal grain and preferably a penetration enhancer, to methods of treating onychomycosis by applying an antifungal composition comprising Lactobacillus species fermented rye, to compositions comprising β-1,3-d-glucan and a penetration enhancer, to β-1,3-d-glucan for use as a direct antifungal agent and to the use of β-1,3-d-glucan for the manufacture of a medication for the treatment of onychomycosis.
CN103007284A Application of HMGCoA reductase inhibitor in preparation of medicine used for treating xerophthalmia The invention relates to an application of an HMGCoA reductase inhibitor in preparation of a medicine used for treating xerophthalmia and belongs to the field of medicines. The inventor finds that a frequently-used lipid regulation medicine, the HMGCoA reductase inhibitor, can obviously prolong SIT time and BUT time and obviously reduce an FLS score when being used for treating the xerophthalmia, and the HMGCoA reductase inhibitor is better than ciclosporin or artificial tears in the aspect of improving the indexes, wherein simvastatin and lovastatin have the best treatment effect. The HMGCoA reductase inhibitor also can be prepared into oral preparation used for treatment or adjuvant therapy of the xerophthalmia. The HMGCoA reductase inhibitor has a definite curative effect and less toxic and side effects, compliance of a patient is high, and clinical ophthalmic drugs are further enriched.
EP1934225A1 Pyrazolo [1,5-a] pyrimidines as protein kinase inhibitors In its many embodiments, the present invention provides a novel class of pyrazolo[1 ,5-a] pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. Formula (I).
CN102198132A Solid preparation of pharmaceutical composition of ketoprofen and omeprazole The invention discloses a liposome preparation of ketoprofen and omeprazole, and the liposome is mainly prepared from, by weight, 5-10 parts of ketoprofen, 1 part of omeprazole, 10-80 parts of hydrogenated yolk lecithin, 3-40 parts of cholesterol and 5-50 parts of Tween 80. And further, a solid preparation of the pharmaceutical composition of ketoprofen and omeprazole is disclosed. The preparation is prepared from the liposome preparation of ketoprofen and omeprazole and other excipients commonly used in pharmacy. According to the invention, the preparation has improved quality and reduced toxic and side effect.
CN101401833A Composition for preventing and/or treating osteoporosis The invention relates to a composition for preventing and/or treating osteoprosis, which comprises yak bone powder, active calcium, vitamin D3, D-Glucosamine Hydrochloride, isoflavones and an epimedium extract. The composition can prevent and/or treat the osteoprosis, has not toxic and side effects, does not induce other pathological changes or diseases.
US7288558 Pharmaceutical composition for treatment for urinary diseases comprising LPA receptor regulator The present invention relates to a pharmaceutical composition for treatment and/or prevention for urinary diseases comprising a lysophosphatidic acid (LPA) receptor regulator. As LPA receptor regulators act on urethra and prostate, compounds acting on this receptor are useful in treating urinary diseases (urinary incontinence, dysuria, etc.). For example, an LPA receptor agonist useful for treatment of urinary incontinence, while an LPA receptor antagonist is useful for treatment of dysuria, ischuria, pollakiuria, nocturia, urodynia and benign prostatic hyperplasia.
WO2009066562A1 Differentiation promoter and/or proliferation promoter for erythrocyte stem cells, use of methionine for preventing or treating senile anemia, and compositions containing methionine It is a first object to develop a remedy efficacious in preventing senile anemia which is frequently observed due to the aging. It is a second object to provide an antiaging drug, which has little side effect and is inexpensive and efficacious, in anticipation of the coming aging society. It is a third object to provide a remedy which is efficacious against anemia caused by myelosuppression, more particularly speaking, anemia occurring as the side effect of the administration of an anticancer agent. It has been clarified for the first time that a drug containing, as the active ingredient, methionine (Met) alone, an amino acid composition containing methionine (Met) together with one or more members selected from among glycine (Gly), serine (Ser) and threonine (Thr) or, furthermore, an amino acid mixture selected from (1) Ile, Trp, Thr, Val, His, Phe,Lys and Leu, (2) Ile, Thr, Val, His, Lys and Leu, (3) Trp, Thr, His, Phe and Lys, and (4) Ile, Trp, Thr, Val, Phe and Leu is capable of ameliorating and healing senile anemia. Thus, preventives for senile anemia, remedies for senile anemia and drugs for preventing cell aging can be provided.
CN1565452A Neurofender, the novel formulation of preventing and delaying aging and death of human cerebral neurocyte The invention discloses a medicinal Neurofender comprising two pharmaceutical constituents of caffeine and P38 enzyme inhibitor, these preparations can reinforce nerve cell film electroactivity, increase LTP forming capability for cells, and lower RAP activation.
WO2011053090A2 Novel 2, 4-pyrimidine derivatives and use thereof The present invention relates to novel 2, 4-pyrimidine derivatives and a use thereof, and more specifically, to pyrimidine derivatives which are effective for systemic lupus erythematosus, a composition for preventing and treating systemic lupus erythematosus comprising the same as an active ingredient and a method for screening the same. The present inventors found novel materials inhibiting surface translocation of gp96 by mimicking a function of AIMP1 which is a molecular anchor for an intracellular residence of gp96, and identified in vitro and in vivo activity of the materials for preventing and treating SLE by alleviating SLE plasma in autoimmune diseases. Therefore, the present invention provides a novel method for screening a therapeutic agent for SLE, and for preventing or treating SLE using the mechanism.
CN102133202A Voriconazole containing tablets The invention relates to voriconazole tablets. The particle size of voriconazole in the tablets is controlled in a range of D(V, 0.9) <= 100 mu m, and the content of a disintegrant accounts for 2-6% of the total weight of the tablets. According to the method provided by the invention, voriconazole tablets with a high dissolution rate, small dissolution difference and small dissolution fluctuation among different batches under different pH conditions can be obtained, thus improving the quality and bioavailability of the voriconazole tablets. The invention adopts a conventional wet granulation process which is simple and suitable for commercial production to prepare the voriconazole tablets.
CN101744825A Cefmenoxime hydrochloride preparation and preparation method The invention provides a cefmenoxime hydrochloride preparation used for injection, which is prepared from the mixture of sterile cefmenoxime hydrochloride and sterile sodium bicarbonate. Sterile cefmenoxime hydrochloride powder is mixed with sterile sodium bicarbonate powder which serves as cosolvent, and the proportion (based on cefmenoxime) of the cefmenoxime hydrochloride and the sodium bicarbonate by weight is 1: 0.15-1: 0.25, preferentially 1: 0.2, that means, 15% of sterile sodium bicarbonate powder (by weight) is added to per l gramme of sterile cefmenoxime hydrochloride powder (based on cefmenoxime). The mixture is blended to be even and then is packed in sterilized cylindroid vials according to labeled amounts through sterile-packing technique, then the cylindroid vials are blocked by tampons and capped, and finally the qualified cylindroid vials are packaged after full inspection. In this way, the cefmenoxime hydrochloride preparation used for injection can be prepared.
CN102526040B Method for preparing composition of mezlocillin sodium and sulbactam sodium for injection in ratio of 4: 1 The invention provides a method for preparing a composition of mezlocillin sodium and sulbactam sodium for injection in a ratio of 4: 1. In the method, conditions and process for mixing the mezlocillin sodium and the sulbactam sodium are studied in a detailed way, the optimal mixing time, temperature and humidity conditions and flowability control indexes are determined, sterile mixing and subpackaging process flows are optimized, and the compatibility and the long-term stability of packaging materials are studied, so that the composition of the mezlocillin sodium and the sulbactam sodium forinjection, with uniform mixing, stable and reliable quality and long-term storage stability, can be obtained.
US20070231395 Solid Pharmaceutical Preparation for Dialysis A solid pharmaceutical preparation for dialysis which does not contain any acetic acid and a production process thereof. The solid pharmaceutical preparation for dialysis contains two pharmaceutical preparations: a solid pharmaceutical preparation (A) composed of particles having an average particle size of about 100 μm to 1,500 μm and containing one or more electrolytes selected from sodium chloride, calcium chloride, magnesium chloride, and potassium chloride, and an organic acid other than acetic acid and/or a salt of the organic acid; and a solid pharmaceutical preparation (B) containing sodium bicarbonate.
CN101259130B Antidiarrheal pharmaceutical composition The invention discloses a composition of an antidiarrheal agent, which consists of the following weight portions of ingredients: 1.5-3 portions of compound diphenoxylate, 2.5-6 portions of prednisone and 5-15 portions of hydrochlorothiazide. The composition of the antidiarrheal agent has clear curative effect, good efficacy, rapid disappearance of diarrhea; diuresis effect of the hydrochlorothiazide is utilized to absorb water and reduce intestinal water, and the anti-inflammatory and anti-infection functions of prednisone are applied to mitigate clinic sympton, the cooperation of these threemedicines accelerates the antidiarrheal speed and relieves the pain of the sufferers. The composition of the antidiarrheal agent has low cost, which is lower than Xieliting by 5-6 times.
CN101947313A Novel effervescent tablet for treating beriberi and preparation process thereof The invention relates to a novel effervescent tablet for treating beriberi and a preparation process thereof. The novel effervescent tablet for treating the beriberi consists of the following materials in part by mass: 0.1 to 0.3 part of trivalent silver ion compound, 0.2 to 0.4 part of keratinase, 0.5 to 5 parts of water soluble keratin, 30 to 60 parts of sodium hydrogen carbonate, 36 to 56 parts of tartaric acid and 40 to 55 parts of alcohol solution containing 5 percent of polyvinylpyrrolidone. The preparation process comprises the following steps of: weighing 0.1 to 0.3 part of trivalent silver ion compound, 0.2 to 0.4 part of keratinase, 0.5 to 5 parts of water soluble keratin, 30 to 60 parts of sodium hydrogen carbonate and 36 to 56 parts of tartaric acid according to the mass ratio; grinding and uniformly mixing; adding 40 to 55 parts of alcohol solution containing 5 percent of polyvinylpyrrolidone as a bonding agent; drying at the temperature of 80 DEG C for 2 to 4 hours; and weighing 0.5 to 2g of mixture, and tableting the mixture under the pressure of 5 to 15 pounds to form the effervescent tablet. The effervescent tablet has the following effects and characteristics of: diminishing inflammation, relieving pain and killing bacteria, dissolving necrotic keratin, repairing skin and rapidly and uniformly releasing active ingredients in water with different temperatures (20 to 80 DEG C).
CN1739524A Lycopene liposome and its prepn process The present invention is lycopene liposome as one new preparation form of lycopene, and the lycopene liposome is prepared through dissolving lycopene organic solution containing lecithin and cholesterol of solvent ethyl ether, dichloromethane or trichloromethane and further film rotating ultrasonic process. The material includes lycopene, cholesterol and lecithin in the weight ratio of 1-5 to 10-25 to 100. The lycopene liposome consists of double liposome molecule layer with inside large water phase monolocular veside of effective grain size 0.7 micron and maximum enclosing rate 52.6 %. The lycopene liposome has target property, no toxicity and no immunogenicity, and may be clinically used to reduce medicine dosage, raise absorption efficiency, lower toxicity, increase the solubility and stability of lycopene and raise bioavailability.
WO2007100304A1 Methods for cancer therapy and stem cell modulation The present invention relates to a method of inducing apoptosis in a tumour cell as well as modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of general formula (I). In general formula A is C or N. R1, R4 and R5 are, independently selected, H or aliphatic, cycloaliphatic, aromatic, arylaliphatic, or arylcycloaliphatic hydrocarbyl groups, that comprise 0 - 3 heteroatoms being N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen, such as F or Cl. R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1 - 8 main chain carbon atoms and 0 - 3 heteroatoms being N, O, S, Si, or a halogen such as Cl or F. Also provided is a pharmaceutical composition for inducing apoptosis in a tumour cell and/or modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The pharmaceutical composition comprises a compound as defined above or a pharmaceutically acceptable salt thereof and a carrier or diluent.
US7544699 Aryl and heteroaryl compounds, compositions, and methods of use This invention provides aryl and heteroaryl compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention may be antagonists, or partial antagonist of factor IX and/or factor XI and thus, may be useful for inhibiting the intrinsic pathway of blood coagulation. The compounds may be useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway.
US20080132567 Alpha-Aminoamide Derivatives Useful in the Treatment of Lower Urinary Tract Disorders Methods of using certain α-aminoamide derivatives to treat lower urinary tract disorders. The therapeutic agents of the invention are able to reduce or even stop the lower urinary tract disorders substantially without side effects.
US20130045966 Method of Lowering Serum Uric Acid Levels With (S)-Tofisopam Enantiomerically-pure (S)-tofisopam is administered to lower serum uric acid levels in a mammal.
EP1959763A1 High-potency sweetener composition with phytosterol and compositions sweetened therewith The present invention relates generally to functional sweetener compositions comprising non-caloric or low-caloric natural and/or synthetic high-potency sweeteners and methods for making and using them. In particular, the present invention relates to different functional sweetener compositions comprising at least one non-caloric or low-caloric natural and/or synthetic high-potency sweetener, at least one sweet taste improving composition, and at least one functional ingredient, such as phytosterols, phytostanols, esters thereof, or combinations thereof. The present invention also relates to functional sweetener compositions and methods that can improve the tastes of non-caloric or low-caloric high-potency sweeteners by imparting a more sugar-like taste or characteristic. In particular, the functional sweetener compositions and methods provide a more sugar-like temporal profile, including sweetness onset and sweetness linger, and/or a more sugar-like flavor profile.
WO2012061926A1 Bisarylsulfone and dialkylarylsulfone compounds as calcium channel blockers The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.
CN101323634A Induced nuclear receptor TR3 expressed cardiac glycoside compounds and use thereof The invention relates to a cardiac glycoside compound for inducing a nuclear receptor TR3 to express. The general formula of the compound of the invention is as follows: wherein, R1 is CH3, CHO or CH2OH; R2 is H or OH; R3 is H or OH; R4 is a linear sugar chain or a branch sugar chain consisted by saccharide. The cardiac glycoside compound of the invention can induce the nuclear receptor TR3 to express, thus being capable of being used as a revulsant to be applied to the preparation of drugs which are used for preventing and treating cancer, hepatitis, atherosclerosis, etc.
CN101972235A Surfactant-containing Lonidamine amorphous multielement solid dispersion and preparation method thereof The invention relates to the fields of chemical pharmacy and pharmaceutic preparation, in particular relating to a compound Lonidamine amorphous multielement solid dispersion and a preparation method thereof. The solid dispersion in the invention is characterized by being prepared from Lonidamine, a surfactant and a solid dispersion carrier, wherein the Lonidamine is dispersed in the solid dispersion carrier in an amorphous mode. The Lonidamine amorphous multielement solid dispersion in the invention has the advantages of non-toxic auxiliary materials, no pollution and simple and convenient operation, and greatly improves the solubility of the Lonidamine, thus enhancing the bioavailability and ensuring good thermodynamic stability of preparations.
WO2005023258A1 Compositions comprising benzo (g) quinoline derivatives and prostaglandin derivatives The present invention relates to a fixed combination of a benzo[g]quinoline derivative and a prostaglandin derivative, and their use as pharmaceuticals, especially for treating glaucoma.
US20070249732 Use of certain phenyl napthyl compounds for protection of neurons and oligodendrocytes in the treatment of multiple sclerosis (ms) Certain biphenyl compounds, including 5-chloro-6-(4-hydroxyphenyl)-2-naphthalenol and 6-(4-hydroxy-phenyl)-2-naphthalene methanol are useful in the treatment of multiple sclerosis on the cellular level of the central nervous system through the protection of the patients' oligodendrocytes and neurons.
CN103536537A Preparation method of lung targeted therapeutic medicine gefitinib PLGA [poly(lactic-co-glycolic acid) microspheres The invention relates to a preparation method of lung targeted therapeutic medicine gefitinib PLGA [poly(lactic-co-glycolic acid) microspheres. The preparation method comprises the following steps: mixing and dissolving gefitinib and PLGA in an organic solvent as a dispersion phase [oil phase (O)]; with lauryl sodium sulfate aqueous liquor as a continuous phase [aqueous phase(W)], slowly injecting the dispersion phase [oil phase (O)] into the continuous phase [aqueous phase(W)] under magnetic stirring to form an oil in water (O/W) type emulsion; continuously stirring for 3 hours, carrying out centrifugal separation on gefitinib PLGA microspheres after the organic solvent is fully volatilized; and washing for 3 times by distilled water and drying to obtain the gefitinib PLGA microspheres. The method is used for preparing the gefitinib PLGA microspheres. The preparation method provided by the invention has the beneficial effects that the gefitinib has high encapsulation efficiency under the condition of ensuring the stability of the gefitinib, the optimal medicament concentration can be maintained in vivo, and the time of medicament effect is prolonged.
WO2005082919A1 Process for isolation and seperation of 3 biological active compounds from aloe vera leaf gel filet and the 3 compounds Aloe vera leaf gel from Aloe barbadensis Miller is one of the most popular herbal material on the market. Most consumers worldwide are familiar with aloe’s use in skin-care products, but aloe can also be used as a beverage. Aloe products for internal use have been promoted for viral infections, wounds, ulcers, diabetes, cancer, headaches, arthritis, immune deficiencies, and many other conditions. The therapeutic effects of aloe gel has been scientifically well researched, and proven. But the major problem lay in the isolation und structure elucidation of the biological active compounds. Many postulate that there are over 100 compounds which work in a synergy to bring about these effects or an acetylated polymannose which has up to date not convinced. This invention has finally provided a method to isolate and elucidate three compounds from aloe gel with clear and independent therapeutic effects. Symbolic for this, is the Veracylglucan C (a oligomalyl hexasaccharide) which up to date has never been found in any other plant on this Planet.
US8389529 Methods and compositions for treating asthma The present application relates to compounds and methods for treating pain, incontinence and other conditions.
CN102987378A Health care product with qi-blood tonifying function The invention discloses a health care product with a qi-blood tonifying function. The health care product is prepared from the following raw materials in parts by weight: 6-24 parts of Chinese angelica, 2-4 parts of donkey-hide gelatin, 3-15 parts of cinnamon, 5-15 parts of codonopsis pilosula, 6-30 parts of astragalus and 10-20 parts of brown sugar. The health care product with the qi-blood tonifying function has the effects of tonifying blood and qi, the qi tonifying contributes to blood tonifying, blood tonifying contributes to qi tonifying, the qi-blood tonifying functions can be realized, and the application range is wide.
CN103550187A Cefdinir capsule and preparation method thereof The invention provides a preparation of a cefdinir capsule and a preparation method thereof. The cefdinir capsule comprises the following components in parts by weight: 90 to 110 parts of cefdinir, 15 to 25 parts of filling agent, 10 to 15 parts of disintegrating agent, 1 to 5 parts of disintegrating accelerant and 1 to 5 parts of other auxiliary materials. The preparation method comprises the following steps: (1) pretreatment of raw auxiliary materials; (2) mixing; (3) filling; and (4) blister packaging.
US8383609 Phosphorus containing heterocyclic compounds, sugar analogues, and compositions having anti-cancer activity containing the same A new anticancer compounds of formula (1) Drugs and pharmaceutical compositions to be used in human or veterinary medicine, which include at least one compound of formula (1). A method of treating and/or preventing cancer in a human or an animal using the compound of formula (1)
CN102058538A Cycloartenyl ferulate solid dispersion and preparation thereof The invention discloses cycloartenyl ferulate solid dispersion, which comprises cycloartenyl ferulate and povidone serving as a carrier material. The invention further discloses a medicinal preparation and a preparation method of the solid dispersion. Experiments prove that the solid dispersion makes obvious technical progress in technical indexes such as dissolution rate, stability, water solubility, bioavailability and the like.
EP1222191B1 Benzodiazepin derivatives, the production and use thereof The invention relates to compounds of formula (I) as well as to the tautomeric forms thereof, possible enantiomeric and diastereomeric forms and the prodrugs thereof, the production and use thereof, whereby the values have the meaning as given in the description.
CN102648897A Ketoprofen macromolecular prodrug polymer microsphere and preparation method thereof The invention relates to a Ketoprofen macromolecular prodrug polymer microsphere and a preparation method thereof. The microsphere comprises the following components: ketoprofen polyvinyl ester and water-soluble macromolecular polymer with a mass ratio of 1-5:10. The preparation method comprises the following steps of: (1) reacting ketoprofen and vinyl acetate to generate ketoprofen vinyl ester, and homopolymerizing the ketoprofen vinyl ester to obtain ketoprofen polyvinyl ester; (2) suspending the ketoprofen vinyl ester in an organic solvent, adding the water-soluble macromolecular polymer, stirring at room temperature, and preparing an electric spraying stock solution; (3) performing electrostatic spraying on the obtained electric spraying stock solution, and performing vacuum drying on a collected sample to obtain the Ketoprofen macromolecular prodrug polymer microsphere. The Ketoprofen macromolecular prodrug polymer microsphere has a fast lasting analgesic effect; and the preparation method is simple and quick, and safe to operate, is completely applicable to relatively large-scale production, and has a good application prospect.
CN103110568A Nanometer drug delivery system carrying tanshinone IIA The invention discloses a nanometer drug delivery system carrying tanshinone IIA, wherein the nanometer drug delivery system is a nanoparticle carrying the tanshinone IIA, which takes methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine polymer modified by valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide as a carrier; the diameter of the nanoparticle is 10-2000nm; and the molecular weight of the polymer is 1.5*103-9.5*106. The molar ratio of the tanshinone IIA and the carrier polymer is 1-60:1-60; the molar ratio of lactic acid in the polymer and the glycolic acid is 1-80:1-80; the molar ratio of the glycolic acid and the lysine is 90-50:10-50; and the molar ratio of the methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine and the valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide is 1-60:1-60. The nanometer drug delivery system carrying the tanshinone IIA can effectively lower the toxicity of the tanshione IIA and increases the targeting of the tanshinone IIA and the treatment effect.
EP0859603B1 Sustained release matrix for high-dose insoluble drugs Sustained release dosage forms of high dose insoluble drugs such as ibuprofen and methods for their manufacture are disclosed.
US20100267671 Compositions and methods for apoptosis modulators The present invention includes and relates generally to compounds which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.
WO2014024077A9 5-(1H-PYRAZOL-4-YL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS The present application relates to novel 5-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to prodrugs, derivatives, polymorphs, pharmaceutically acceptable salts and compositions comprising the said novel 5-(1H-pyrazol-4-yl)-1H- pyrrolo[2,3-b]pyridine compounds and their derivatives and their use in the treatment of various disorders.
US20080254031 Nucleotide sequences coding tumor antigens for use as diagnostic tool in detection and staging of cell proliferative disorders Genes and variant RNAs that are differentially expressed in human colon tumor tissues compared with normal colon tissue and the corresponding proteins are identified. These genes and the corresponding antigens are suitable targets for the treatment, diagnosis or prophylaxis of colon cancer.
US7025975 Galenical formulations A pharmaceutical composition containing macrolide, e.g. a rapamycin compound in an emulsion preconcentrate or microemulsion preconcentrate for oral administration. The carrier medium for the rapamycin compound includes a hydrophilic phase, a lipophilic phase and a surfactant. The composition is stable and provides high absorption efficiency.
US20070259889 Protein Binding Compounds The present invention provides a prodrug compound comprising a therapeutically effective moiety coupled via a metabolically cleavable bond to a blood protein binding moiety.
EP2445908A1 Disubstituted benzamide derivatives as glucokinase (gk) activators The invention relates to disubstituted benzamide derivatives of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating type II diabetes using the compounds of the invention.
CN103193677A Polymorphic form of methocarbamol disodium phosphate and preparation method thereof The invention relates to a polymorphic form of propanediol, 3- (2- methoxyphenoxy)-, 1-carbamate disodium phosphate (methocarbamol disodium phosphate) and a preparation method and application thereof. The polycrystalline has an X-ray powder diffraction pattern shown as Figure 1, nuclear magnetic resonance absorption patterns shown as Figure 2 and Figure 3, a thermogravimetry-differential thermal analysis curve shown as Figure 4, mass spectrum peaks shown as Figure 5 and Figure 6 and an infrared spectral absorption curve characterization result shown as Figure 7. The polycrystalline can be used for preparing medicaments for treating muscle strain, lumbar muscle strain and sciatica. The polymorphic form powder is fine, uniform in dispersion and high in stability, the water solubility of the polycrystalline powder is 1:2, and the crystallization process is simple, facilitates production, transportation and storage and meets the requirements of medicament preparation.
US7241778 E.g., 1-[4-(1-Isopropyl-piperidin-4-yloxy)-benzyl]-piperidine and 1-[4-(1-Isopropyl-piperidin-4-yloxy)-benzyl]-azepane; these compounds modulate the activity of the histamine receptor, specifically the H3 receptor, without the inherent problems associated with the presence of an imidazolyl moiety Substituted non-imidazole aryloxypiperidine compounds, compositions containing them, and methods of making and using them to treat or prevent histamine-mediated conditions.
US7560479 3,6-Disubstituted azabicyclo hexane derivatives as muscarinic receptor antagonists This invention relates to derivatives of 3,6-disubstituted azabicyclo hexanes. The compounds of this invention can function as muscarinic receptor antagonists and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors.
WO2005011680A1 Use of angiotensin ii receptor antagonists, especially telmisartan, in order to increase insulin sensitivity The invention relates to the use of angiotensin II receptor antagonists for the treatment of people who have been diagnosed with type 2 diabetes mellitus, or are thought to have prediabetes, in order to prevent diabetes or for the treatment of metabolic syndrome and the resistance of insulin in patients having normal blood pressure.
CN103432117A Application of methysticin The invention discloses the application of methysticin used as a histidine kinase VicK inhibitor in vitro or application of methysticin in preparation of the histidine kinase VicK inhibitor. The methysticin has a certain antibacterial effect on in-vivo streptococcus pneumoniae and clinical penicillin resistant streptococcus pneumoniae. Moreover, the medicament has a good antibacterial effect on streptococcus pneumoniae after being combined with penicillin, and has obvious bacteriostasis on staphylococcus aureus.
WO2014045310A1 Pyrimido[5,4-d]pyrimidine or pyrimidine derivatives compounds and uses thereof in the treatment of cancer The present invention concerns pyrimido[5,4-d]pyrimidine or pyrimidine derivatives compounds and uses thereof in the treatment of overexpressing H-prune cancer, i.e. metastatic cancer.
CN1651016A Biological polysaccharide polymer lichen inhibiting film agent and its preparation method A medicine in the form of film for treating tinea pedis, tinea manuum and jock itch is prepared from the mixture of biologic polyoses chosen from sand sage polyose, xanthan polyose and guar polyose, the extracts of 4 Chinese-medicinal materials including liquorice root, mint, etc. and the mixture of benzoic acid, resorcinol, phenol and salicylic acid.
US20110281937 Methods and compositions for treating neuropathic and neurodegenerative conditions Disclosed herein are engineered zinc finger proteins which modulate transcription of the gene encoding vascular endothelial growth factor-A (VEGF-A) and other genes encoding products with neurotrophic activities. Also disclosed are methods for the use of these engineered zinc finger proteins in the treatment of neuropathy (including diabetic neuropathy), and other types of neural injury and neurodegeneration.
WO2009039460A3 Co-administration of pimavanserin with other agents As disclosed herein, co-administration of pimavanserin with an agent that ameliorates one or more cholinergic abnormalities can have a synergistic effect on the efficacy of the agent. Disclosed herein are compositions which include pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities. Also disclosed herein are methods for ameliorating or treating a disease condition characterized by one or more cholinergic abnormalities that can include administering pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities.
CN103156880A Pharmaceutical composite containing colloidal bismuth pectin The invention provides a pharmaceutical composite for treating gastric ulcer. The pharmaceutical composite comprises colloidal bismuth pectin and furazolidone which have the effect of synergistic treatment.
US7169787 e.g., N-(4-pyridylmethyl)-1-cyclopropylmethyl-7-azaindole-3-carboxylic acid amide The invention relates to new 7-azaindoles, their use as inhibitors of phosphodiesterase 4 and to methods for their synthesis.
US8404633 CD5 pharmaceutical compositions for the treatment of infectious and inflammatory processes of fungal origin The present invention refers to pharmaceutical compositions comprising the soluble CD5 ectodomain and its use for the prevention and/or treatment of fungal infections and/or fungal sepsis, as well as inflammatory disorders of fungal origin.
CN101230055A Lovastatin analogue as well as preparation method and uses thereof The invention relates to a lovastatin structure analog. The structure is shown in formula A. The molecular formula is C24H34O5, and the molecular weight is 402.5. The preparation of a compound adopts lovastatin as the raw material, basic hydrolysis, cyclization, protecting group application, and esterification reaction with 2-methyl-2-crotonyl chloride are all performed to lovastatin, and then the lovastatin structure analog is obtained through deprotection in acidic condition. The results of experimental rat high blood fat model experiments show that the compound has a certain function for reducing blood cholesterol and low density lipoprotein, and can be used for preparing medicines for reducing blood fat, in addition, the compound can be used as a platform for further deriving and synthesizing other lovastatin analogs.
CN1593400A Anticancer methylcantharidinimide tablet and its preparation method The invention discloses an antineoplastic methylcantharidinimide tablet whose preparation comprises cantharis selection, disintegrating, cantharidin extraction, cantharidin degreasing, methylcantharidinimide synthesizing, methylcantharidinimide refining, methylcantharidinimide tablet pressing, sterilizing, and packaging.
EP2231189A1 Drug delivery system for administration of poorly water soluble pharmaceutically active substances This invention relates to a drug delivery system for administration of poorly water soluble pharmaceutically active substance, a pharmaceutical composition comprising such a drug delivery system, and a method for the preparation of such a drug delivery system. The invention also relates to a method for controlling the particle size and/or particle shape and/or particle size distribution in such a drug delivery system, and to a method for increasing the drug loading capacity of the particles. Furthermore the invention also relates to the use of such a drug delivery system for the preparation of a medicament for the treatment of cancer.
WO2014052379A1 Substituted cyclopropyl compounds Substituted cyclopropyl piperidinyl compounds and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-1 19. Pharmaceutical compositions and methods of treatment are also included.
WO2014093475A1 Methods for treating parkinson's disease using aminopyridines Provided herein are methods and compositions for treatment of patients with Parkinson's disease and, in particular, motor impairments in patients with Parkinson's disease, using an aminopyridine.
US20080021080 4-(3-{[4-(4-Ethyl-3-methyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phenyl]thio}phenyl)tetrahydro-2H-pyran-4-carboxamide (Compound No. 1); bronchial asthma, chronic obstructive pulmonary disorder, arthritis, type I diabetes, multiple sclerosis, allograft rejection, psoriasis, inflammatory bowel disease The present invention relates to 5-lipoxygenase inhibitors. Compounds disclosed herein can be useful in the treatment of bronchial asthma, chronic obstructive pulmonary disorder, arthritis, type I diabetes, multiple sclerosis, allograft rejection, psoriasis, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, urticaria, atopic dermatitis, allergic rhinitis, other inflammatory and autoimmune diseases. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as 5-lipoxygenase inhibitors are also provided.
CN103113371A Acyclovir eutectic and preparation method thereof and preparation The invention discloses an acyclovir eutectic, a preparation method of the acyclovir eutectic, and a preparation. The x-ray powder diffraction of the acyclovir-glutaric acid eutectic has characteristic peaks in the diffraction angles 2 theta at 8.108, 10.890, 13.975, 14.421, 16.125, 16.611, 18.700, 20.468, 21.504, 21.887, 22.495, 23.208, 24.143, 25.015, 26.069, 27.410, 28.506, 29.135, 30.901, 32.524, 32.972, 34.126, 35.609, 36.049 and 37.153. According to the preparation, two ways, namely, a way of adding an organic solvent and grinding and a way of dissolving in the organic solvent, settling, filtering and drying, are respectively adopted, and therefore the higher-purity acyclovir-glutaric acid eutectic is successfully prepared. The preparation method has the advantages that few solvents are needed in the production process, the production cost is low, and less pollution is brought to the environment. Compared with the acyclovir, the acyclovir-glutaric acid eutectic disclosed by the invention has the advantages of being higher in permeability and stable in performance, and shows more advantages in the application of preparing a transdermal absorption preparation.
CN1903222A Method and recipe for preparing cockroach band aid An adhesive bandage for promoting growth of granulation tissue, speeding up the repair to damaged tissue and relieving inflammation features that its active components include the extract of roach. Its prescription and preparing process are also disclosed.
CN103536598A Application of compound in preparation of drug for treating liver cancer The invention discloses application of a compound in preparation of a drug for treating a liver cancer. The compound is Asperterpenols A, and belongs to the technical field of new use of a drug. In vitro microwave theory and techniques (MTT) anti-tumor activity evaluation shows that the Asperterpenols A has a significant inhibiting effect on growth of human hepatocellular carcinoma cells HEPG2, MHCC-LM3, BEL-7402 and HUH-7. Therefore, the Asperterpenols A can be applied to preparation of an anti-hepatoma drug, and has excellent development and application prospects. The use of the Asperterpenols A related to the invention in preparation of the drug for treating the liver cancer is disclosed for the first time; furthermore, the Asperterpenols A is strong in inhibitory activity on a hepatoma carcinoma cell, and has significant progress.
CN103705944A Preparation method and application of folic acid-modified nano-diamond targeting medicine The invention provides a preparation method of a folic acid modified nano-diamond targeting medicine (ND-PEG-FA-DOX) and the medicine prepared with the method. The medicine acts on human hepatoma carcinoma cells (HepG2), the cells are treated different inhibitors and free folic acid at low temperature,, and the result indicates that the medicine is energy-dependent, and enters cells through a clathrin-determined and folic acid receptor-mediated mechanism. The cytotoxicity of the medicine is detected with an MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay, the result indicates that the medicine has a targeting anti-tumor effect on cancer cells. An experiment for study the effects of the medicine and independent adriamycin along on the activity of tumor cells indicates that the medicine has the characteristics of slow release of medicine. Therefore, by using the ND-PEG-FA-DOX, the toxic and side effects of chemotherapeutics on normal cells can be reduced, and the killing ability of the chemotherapeutics for the tumor cells is improved. The ND-PEG-FA-DOX can be applied in preparing targeting anti-tumor medicines.
CN101700232A Cefprozil submicron emulsion solid preparation and new application thereof The invention relates to a cefprozil submicron emulsion solid preparation and new application thereof in the preparation of medicine for treating acute plasma cell mastitis. The cefprozil submicron emulsion granule comprises cefprozil, yolk lecithin, poloxamer 188 and deoxysodium cholate with the weight ratio of 1:2.3-14:1.2-8:0.8-10.
US8633313 Heterocyclic compounds and their uses Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
WO2013192517A3 Compounds for treating infectious diseases The present invention provides compounds of Formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting fungal or parasitic growth. The compounds are useful as inhibitors of glycosylphosphatidylinositol (GPI)-anchor biosynthesis, in particular, as inhibitors of fungal Gwtl activity. The present invention further provides methods of using the compounds described herein for treating fungal or parasitic infections. The compounds can also be used as biological probes to study the effects of inhibiting Gwtl activity.
WO2012031017A1 CRYSTALLINE FORMS OF A FACTOR Xa INHIBITOR Provided herein are crystalline forms of a maleate salt of betrixaban, compositions and methods of preparation or use thereof.
US20090075930 for treating leukemia The present application describes deuterium-enriched nelarabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20100227936 Treatment of microbial infections with compounds that inhibit 4-hydroxyphenylpyruvate dioxygenase Methods of inhibiting phagolysosomal fusion in patients infected with a microorganism involve the administration of a 4-hydroxyphenylpyruvate dioxygenase (HPPD)-inhibiting compound, such as 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione (NTBC) to the patient. A HPPD-inhibiting compound administered in an amount effective to enhance phagolysosomal fusion in the macrophages or neutrophils of the patient reduces or treats the infection. Methods for treating bacterial infections by administering a HPPD-inhibiting compound and reducing the production of pyomelanin or melanin in microorganisms are disclosed.
US20090298911 Short interfering RNA sequences for prevention and treatment of viral infection; viricides The present invention relates to an siRNA (small interfering RNA) having antiviral activity against nonpolio enteroviruses, and a pharmaceutical composition comprising same as an active ingredient for preventing and treating diseases caused by nonpolio enterovirus infection.
US20100204174 Novel active ingredient in cicatrization and use thereof The present invention relates to the use of a known compound as an agent for promoting and/or accelerating fibroblast proliferation and/or differentiation and, consequently, cicatrization. This compound is a copolymer of a 2-methyl-2-[(1-oxo-2-propenyl)amino]-1-propanesulphonic acid salt and of propenoic acid 2-hydroxyethyl ester. It may be used alone or in combination with other active substances for inducing or accelerating cicatrization. This compound, alone or in combination with another active substance, may be administered directly on the wound and the surrounding area or the mucous membranes, by topical application. It may also be used ex vivo, in particular for generating cells for skin grafts.
US20120289600 Optimized strains of yarrowia lipolytica for high eicosapentaenoic acid production Engineered strains of the oleaginous yeast Yarrowia lipolytica capable of producing greater than 50 weight percent of eicosapentaenoic acid [“EPA”], an ω-3 polyunsaturated fatty acid, in the total oil fraction are described. These strains over-express heterologous Δ9 elongases, Δ8 desaturases, Δ5 desaturases, Δ17 desaturases, Δ12 desaturases and C16/18 elongases, and optionally over-express diacylglycerol cholinephosphotransferases. Preferred gene knockouts are also described. Production host cells, methods for producing EPA within said host cells, and products comprising EPA from the optimized Yarrowia lipolytica strains are claimed.
CN103191296A Enema medicine for treating night crying of infants The invention discloses an enema medicine for treating night crying of infants. The enema medicine comprises the following raw materials in proportioning by weight: 3-20g of berufkraut, 2-15g of radix ophiopogonis, 6-20g of honey-fried licorice root, 5-30g of myrrh, 2-20g of radish seed, 2-20g of shaved cinnamon bark, 2-20g of poria cocos and 10-20g of borneol. The enema medicine has good effects of clearing heat and removing toxicity, resisting bacteria and easing pain, tonifying spleen and harmonizing stomach, and treating abdominal distension and abdominal pain and can be used for effectively treating the night crying of infants.
EP1372621B1 Novel use of tyrosine kinase frk inhibitor The present invention relates to a novel use of a tyrosine kinase inhibitor or blocking agent. More precisely, it relates to use of an inhibitor of tyrosine kinase for production of a drug for prevention/treatment of type I diabetes mellitus, wherein the inhibitor is a GTK (BSK, IYK, FRK, RAK) tyrosine kinase. The invention also relates to use of FRK (or its equivalents) or the gene encoding the same, in an assay to screen for compounds interfering with FRK activity in pancreatic beta -cells. Furthermore, the invention relates to a method of prevention/treatment of type I diabetes mellitus, comprising administration of an inhibitor against a FRK tyrosine kinase in pancreatic beta -cells to type I diabetic patients.
WO2008019302A1 Pyrazolylphenyl and pyrrolylphenyl inhibitors of lta4h for treating inflammation Two chemical genera of pyrazolylphenyl and pyrrolylphenyl derivatives are disclosed. They have the general formula (I) and (II). In these compounds ring (a) is a pyrazole or pyrrole; Q is selected from the group consisting of a direct bond, O, S, SO, SO2, NR1, CH2, CF2, and C(O); HET is a 4-7-membered saturated nitrogenous heterocycle; and taken together ZW is H or Z is (CH2)1-10 in which one or two (CH2) may optionally be replaced by -O-, NR1-, SO, S(O)2-, -C(=O)- or -C=O(NH)-; and W is hydrogen, acyl, hydroxyl, carboxyl, amino, carboxamido, aminoacyl, COOalkyl, -CHO, heterocyclyl, substituted aryl or substituted heterocyclyl. The compounds are inhibitors of LTA4H (leukotriene A4 hydrolase). They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
CN101219123A Tea polyphenol pellet and method for preparing the same The invention provides a tea polyphenols micro-pill that is prepared from tea polyphenols and pharmaceutical adjuvant, which is characterized in that the pharmaceutical adjuvant is an excipient and a bonding agent. The tea polyphenol micro-pill comprises (by weight percentage) that: tea polyphenols 20-80 percent, the excipient 15-79 percent and the bonding agent 1-5 percent. The tea polyphenols micro-pill can be made into sustained-release preparation or enteric-coated preparation. The pharmacological experiment indicates that the tea polyphenols micro-pill of the invention has good effect on radioresistance, anti-aging, etc.
CN102973879A Calculi treatment mixture and preparation method thereof The present invention relates to a calculi treatment mixture and a preparation method thereof. The preparation method comprises: (1) carrying out deep frying on English walnut seed by using edible oil to a crisp state, pounding, and mixing the pounded English walnut seed and white granulated sugar to obtain calculi treatment English walnut seed medicinal instant granules; (2) cleaning lysimachia and herba pyrrosiae; (3) weighing 50-60% by weight of English walnut seed, 15-25% by weight of white granulated sugar, 30-60% by weight of lysimachia, 10-20% by weight of herba pyrrosiae, 10-20% by weight of talc, 10-15% by weight of akabia stem, 10-15% by weight of oriental waterplantain tuber, 5-10% by weight of wenchow turmeric root tuber, 10-20% by weight of japanese climbing fern spore, 5-15% by weight of chicken's gizzard-membrane, 3-7% by weight of licorice root, and 5-15% by weight of asiatic plantain seed; (4) respectively adding water to various components (except English walnut seed and white granulated sugar), boiling two times at a temperature of 100 DEG C, mixing the two obtained solutions, and carrying out cooling and then packaging to obtain a calculi treatment liquid agent; and (5) mixing the calculi treatment English walnut seed medicinal instant granules and the calculi treatment liquid agent to obtain the calculi treatment mixture. The calculi treatment mixture has the following advantages that: a treatment effect is rapid, wherein an effect is provided in the next day after taking the calculi treatment mixture; a use range is wide, wherein the calculi treatment mixture has functions of diuresis promoting, stranguria dredging, heat clearing, calculi removing and the like, and is suitable for treatment of kidney stones, ureteral stones, bladder stones and other urinary system stones; and drug sources are wide, and price is low.
US7691846 blood coagulation factor (trypsin-like serine protease enzymes) inhibitor; 1-(3-amino-1,2-benzisoxazol-5-yl)-5-{[5-(2-oxo-1-piperidinyl)-2,3-dihydro-1H-indol-1-yl]carbonyl}-1H-pyrazole-3-carboxamide; anticoagulant; cardiovascular thromboembolic disorder transient ischemic attack, stroke, atherosclerosis The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4 I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
EP2050438A1 Spherical crude granule and method for production thereof The characteristic in being coated with film of spherical elementary granules is improved by adjusting a short/long diameter-ratio distribution coefficient to a specific value.
CN102512367A Formula of novel docosahexaenoic acid (DHA) fat emulsion preparation and preparation method thereof The invention discloses a formula of a novel docosahexaenoic acid (DHA) fat emulsion preparation and a preparation method thereof. The novel preparation main comprises DHA, an emulsion, soybean oil or other refined oil as an oil-soluble diluent, oleic acid or oleate as auxiliary emulsification, vitamin E or a vitamin E derivative as antioxidation, an ion chelating agent and glycerol or micromolecule sugar as an isotonic adjusting agent. A variety of methods are used alone or are used together to prepare the DHA fat emulsion preparation.
US20080300199 Antibacterial 1,4,5-substituted aminoglycoside analogs The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.
EP1688418A2 Chemokine receptor antagonists and methods of use thereof Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: formula (1) or physiologically acceptable salt thereof.
US20060263305 Using azithromycin antibiotic In a biofilm removing agent containing a macrolide antibiotic for removing a biofilm formed by periodontal pathogens, the macrolide antibiotic is 15-membered ring azithromycin.
EP2762144A1 Inhibitor for corneal epithelial cell death, inhibitor characterized by combining hyaluronic acid and flavin adenine dinucleotide A combination of hyaluronic acid or a salt thereof and flavin adenine dinucleotide or a salt thereof can be an inhibitor for corneal epithelial cell death induced by ultraviolet irradiation and/or dryness because it significantly inhibits the decline of the number of living cells in corneal epithelial cells induced by ultraviolet irradiation or dryness.
US8647820 Circular dumbbell decoy oligodeoxynucleotides (CDODN) containing DNA bindings sites of transcription The present invention provides a circular dumbbell oligodeoxynucleotide (CDODN) comprising two loop structures and a stem structure, wherein the stem structure comprises a nucleotide sequence capable of binding the DNA-binding domain of a transcriptional factor. The present invention further provides a pharmaceutical composition comprising said CDODN. The pharmaceutical composition can be used for treating and/or preventing a disease or disorder related to such a transcriptional factor. The present invention also provides a method for treating and/or preventing a disease or disorder related to such a transcriptional factor, comprising administering to the subject a therapeutically effective amount of a CDODN comprising two loop structures and a stem structure, wherein the stem structure comprises a nucleotide sequence capable of binding the DNA-binding domain of the transcriptional factor.
CN101732291A Application of dimethyl sulfoxide in preparing anti-aging products The invention discloses a new application of dimethyl sulfoxide which is applied to preparing anti-aging products and nematoid life prolonging agents. The invention utilizes the biology having the mode of nematoid, detects by using a whole animal experiment, observes the influence of the dimethyl sulfoxide on the life of nematoid and finds that 0.5 to 2 percent of dimethyl sulfoxide can obviously prolong the average life and the maximum life of the nematoid.
US20120156138 Methods and Compositions for the Treatment of Medical Conditions Involving Cellular Reprogramming The present invention provides a variety of nucleic acid based therapeutics and methods of use thereof which are effective to beneficially reprogram diseased cells such that they exhibit more desirable phenotypes. Also provided are compositions and methods to reprogram normal cells for medical and commercial purposes.
CN102961338A Polyferose controlled-release pellet and preparation method thereof The invention provides a polyferose controlled-release pellet and a preparation method thereof. The polyferose controlled-release pellet consists of a pill core and a controlled-released film cover, wherein the medicine-contained pill core consists of 350 parts of polyferose, 1-50 parts of adhesives and 50-250 parts of blank pill cores; the controlled-released film cover consists of 5-50 parts of controlled-release materials, 0.5-10 parts of pore-foaming agent and 0.5-10 parts of plasticizer. According to the polyferose controlled-release pellet, drugs can be released durably and slowly, the blood concentration is stable, the fluctuation is slight, the phenomenon of blood concentration peak of quick-acting preparation can be avoided, the strong stimulation on the gastrointestinal tract caused by overhigh local drug concentration can be avoided, and the side effect to the gastrointestinal tract is small; the effective lasting time is long, people only need to take the pellet for one time every day, and can take the pellet conveniently; a human body can absorb the pellet effectively, the absorbing individual difference is small, and the good effect can be achieved; and the preparation method is simple, the reproducibility is good, and the pellet is suitable for industrial production.
US7122543 Substituted benzoic acid derivatives having NF-κB inhibiting action A substituted benzoic acid derivative which is represented by the following formula (I) and has an NF-κB inhibiting action (in the formula, R3, R4 and R5 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an alkoxy group having 1 to 6 carbon(s); R9 and R10 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an acyl group having 2 to 11 carbons); R2 represents an optionally-substituted aromatic hydrocarbon group or an optionally-substituted heterocyclic group; and X represents a carboxyl group which may be esterified or amidated)
US20110294877 Transition metal complexes of bis[thiohydrazide amide] compounds The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thiohydrazide amide] is represented by Structural Formula (I), or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. In one embodiment, the compound is represented by Structural Formula (II), or a prodrug, isomer, ester, salt, hydrate, solvate or polymorph thereof. The present invention also provides a pharmaceutical composition comprising the compound of the invention and method of use thereof.
US20110189213 Mybl2 epitope peptides and vaccines containing the same Peptide vaccines against cancer are described herein. In particular, the present invention describes epitope peptides derived from MYBL2 that elicit CTLs. The present invention also provides established CTLs that specifically recognize HLA-A24 positive target cells pulsed with the peptides. Antigen-presenting cells and exosomes that present any of the peptides, as well as methods for inducing antigen-presenting cells are also provided. The present invention further provides pharmaceutical agents containing the MYBL2 polypeptides or polynucleotides encoding thereof, as well as exosomes and antigen-presenting cells as active ingredients. Furthermore, the present invention provides methods for treating and/or prophylaxis of (i.e., preventing) cancers (tumors), and/or prevention of postoperative recurrence thereof, as well as methods for inducing CTLs, methods for inducing anti-tumor immunity, using the MYBL2 polypeptides, polynucleotides encoding the polypeptides, exosomes or antigen-presenting cells presenting the polypeptides, or the pharmaceutical agents of the present invention. The cancers to be targeted include, but are not limited to, testicular tumor, pancreatic cancer, bladder cancer, non-small cell lung cancer, small cell lung cancer and esophageal cancer.
US20110098265 Methods for reducing cravings and impulses associated with addictive and compulsive behaviors This document provides methods and materials related to managing weight, supporting appetite control, and controlling cravings associated with smoking reduction or cessation regimens and/or nicotine reduction or cessation regimens. For example, compositions comprising an agent to support acetylcholine and an agent to support one or more biogenic amines, and methods for using such compositions for craving and appetite control are provided. Methods and materials to reduce cravings associated with the reduction or cessation of the use of chemical substances (e.g., drugs of abuse, including opioids, cocaine, methamphetamine, cannabis, alcohol), and to reduce cravings associated with addictive and/or compulsive behaviors (e.g., gambling, sex, and repetitive behaviors) are also provided.
CA2187626C Aav-mediated delivery of dna to cells of the nervous system The invention relates to a method of delivering exogenous DNA to a target cell of the mammalian central nervous system using an adeno-associated virus (AAV)-derived vector. Also included in the invention are the AAV-derived vectors containing exogenous DNAwhich encodes a protein or proteins which prevent or treat nervous system disease, and a method of preventing or treating such disease.
EP1627639A2 Use of COX-2 inhibitors for the treatment of affective disorders The present invention relates to the use of a COX-2 inhibitor in the preparation of a medicament for the treatment of affective disorders. Particular affective disorders include depression, depressive episodes, recurring depressive episodes, manic episodes and bipolar affective disorders. The COX-2 inhibitor may be selected from inter alia celecoxib, rofecoxib, meloxicam, piroxicam, deracoxib, parecoxib, valdecoxib, etoricoxib, and so forth, as well as pharmaceutically acceptable salts, prodrugs or mixtures thereof.
CN103037841A Intravenous curcumin and derivatives for treatment of neurodegenerative and stress disorders Liposomal formulations and polymer conjugates of curcumin, curcumin analogues and derivatives thereof for parenteral administration are disclosed herein. The formulations are effective in the treatment of progressive supranuclear palsy, Alzheimer's disease (AD), Parkinson's disease (PD), Tauopathies or stress disorders including Post Traumatic Stress Disorder (PTSD). Curcumin crosses the blood brain barrier, localizes in the hiTppocampus and striata, prevents stress-induced neuronal cell damage, and stimulates neurogenesis and remediation of damaged neural circuits.
US20130023559 Alcohol free formulation of argatroban An aqueous formulation of argatroban and of related compounds is disclosed along with a reconstitutable formulation, each of which is substantially, if not totally alcohol free. The formulations are also substantially free, if not totally free, of mono-, di-, and oligo-saccharides. An especially preferred embodiment is a ready-to-use 1 mg/ml injectable dosage form having argatroban, lactobionic acid, and methionine.
US20110105453 Superoxide Dismutase Mimics For The Treatment Of Optic Nerve And Retinal Damage Methods for preventing and treating damage to the optic nerve and/or retina by the use of SOD mimics, particularly pentaazacycle Mn(II) complex SOD mimics, are disclosed.
WO2009119785A1 Method for purifying ethynylthymidine compound Disclosed is a method for purifying 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine or a base salt thereof, which is characterized in that a crystal of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine or a base salt thereof is deposited by bringing a solution containing a base salt of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine and a base salt of a diastereomer of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine into contact with a solvent in which base salts of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine are poorly soluble. The method can efficiently and commercially advantageously purify 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine or a base salt thereof, which is useful as a pharmaceutical product.
CN101433541A Pharmaceutical composition containing beta2 agonists and steroids, and uses thereof The invention belongs to the medicine technical field, and relates to a pharmaceutical composition of a beta2 receptor agonist and steroid and application thereof, in particular to a pharmaceutical composition of tranditerol or salt thereof, or mabuterol or salt thereof, and fluticasone propionate and application thereof, wherein the mixture ratio of the tranditerol or the salt thereof to the mabuterol or the salt thereof to the fluticasone propionate is 10 to 1-1 to 10,000; and the composition can be a composition which can be atomized in respirable mode, and can be used for preparing an aerosol inhalant and an aerosol. The composition can be prepared into capsules and other formulations with other auxiliary materials after the composition is prepared into dried powder with pharmaceutically acceptable carriers. The composition can significantly improve pulmonary function, and can control obstructive or phlogistic airway diseases or slow down depravation of the diseases. The composition can be used for preparing medicaments for salving and treating the obstructive or phlogistic airway diseases.
WO2011141847A1 An improved process for the preparation of meropenem The present invention provides an improved process for the preparation of methyl carbapenem derivative of formula (I) or its pharmaceutically acceptable salts or hydrates thereof in a pure form.
CA2590556A1 Process for preparing tolterodine tartrate The invention encompasses processes for making tolterodine tartrate.
WO2014057068A1 Liquid pharmaceutical composition of factor vii polypeptide The invention concerns a liquid pharmaceutical composition comprising: A Factor VIIa polypeptide; A buffering agent suitable for keeping pH in the range of from about 5.5 to about 8.5; and An active site stabilizing agent, which is a compound exhibiting a Fit value >0 in the pharmacophore model described by the Pharmacophore Model and Methods Description when using the parameter settings described by the Pharmacophore Model and Methods Description, or a pharmaceutically acceptable salt of said compound.
CA2639525A1 Topical composition for the protection and/or treatment of radiation related skin damages There is provided a topical composition for the protection and/or treatment of radiation related skin damages comprising from 18.4% to 68% by volume of active principles comprising anti-oxidants, moisturizers, humectants, emollients, anti-inflammatory agents, healing promoting agents and dermal circulation enhancers in from 81.6% to 32% by volume of a pharmaceutically acceptable carrier.
WO2008056188A3 Novel compounds and methods for their production The present invention relates to ansamycin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases or a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine.
CN102218071A Micronized deflazacort oral preparation and preparation method thereof The invention discloses a deflazacort oral preparation and a preparation method thereof. The deflazacort oral preparation comprises micronized deflazacort, wherein 50 to 100% of deflazacort particles have particle sizes less than or equal to 50 micrometers. The micronized deflazacort oral preparation is prepared from 2 to 40% of micronized deflazacort, 50 to 95% of one or more fillers, 1 to 10% of one or more disintegrants, 1 to 10% of one or more binders and 0.3 to 1% of a lubricant. The micronized deflazacort oral preparation is characterized in that through a process of mixing raw materials and lactose in an equal amount increasing way, a uniformity degree and a dissolution rate of raw materials can be improved; micronized deflazacort can improve a dissolution degree in vitro; and selected and combined raw materials are suitable for drug molding and have a high stability and good drug effects.
WO2005026132A1 cAMP-SPECIFIC PHOSPHODIESTERASE INHIBITOR [PROBLEMS] The invention aims at providing drugs containing as the active ingredient benzoguanamine derivatives or pharmaceutically acceptable salts thereof which exhibit specific inhibitory activities against cAMP phosphodiesterase. [MEANS FOR SOLVING PROBLEMS] cAMP-specific phosphodiesterase inhibitor, containing as the active ingredient benzoguanamine derivatives represented by the general formula (I) or pharmaceutically acceptable salts thereof; and preventive or therapeutic drugs for bronchial asthmas including atopic asthma and so on, containing as the active ingredient benzoguanamine derivatives represented by the general formula (I) or pharmaceutically acceptable salts thereof: (I) wherein R1 and R2 are each independently hydrogen or halogeno.
WO2014069836A1 Histamine receptor antagonist composition containing policosanol as active ingredient The present invention provides a novel use of policosanol as a histamine receptor antagonist. Policosanol is used as a natural antihistamine and can be used for preventing or treating allergic rhinitis, inflammatory bowel diseases, asthma, bronchitis, vomiting, stomach and duodenal ulcer, gastoesophegal reflux diseases, sleep disturbance, anxiety, and depression, and has the advantages of further reducing sleep latency and increasing sleep time. Policosanol is a natural product derived from rice bran, sugar cane, wheat, sorghum and the like, and does not cause side effects such as cognitive impairment, resistance, or dependence even after long-term use.
US20120114604 Combinations for HCV Treatment The present invention relates to co-administering a Hepatitis C virus NS3/4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The combination acts by interfering with the life cycle of the hepatitis C virus and is therefore useful as an antiviral therapy. As such, the combination may be used for treating or preventing Hepatitis C infections in patients. The invention also relates to compositions comprising the combination of inhibitors. The invention also relates to kits and pharmaceutical packs comprising a Hepatitis C virus NS3/4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The invention also relates to processes for preparing these compositions, combinations, kits, and packs.
EP2408755A2 Psma-targeting compounds and uses thereof Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.
CN1771983A Azithromycin dripping pill and its prepn The present invention discloses one kind of antibiotic medicine, and aims at providing one kind of orally taken azithromycin dripping pill with high bioavailability, fast medicine release, fast acting, high medicine content, easy taking, low cost and production process without pollution. The azithromycin dripping pill is prepared with azithromycin as medicine material and medicine carrier as matrix.
US20080193550 conjugated linoleic acid; treat, prevent conditions associated with leukocyte infiltration, eosinophilia, IgE secretion, airway remodelling, bronchoconstriction, mucus hypersecretion, asthma; injection, ingestion, inhalation, topical The present invention relates to use of c-9, t-11 CLA or a salt, ester or precursor thereof or CLA-enriched milk fat comprising milk fat enriched with c-9, t-11 CLA or a salt, ester or precursor thereof for treating or preventing conditions such as those associated with one or more of leukocyte infiltration, eosinophilia, IgE secretion, airway remodelling, bronchoconstriction and mucus hypersecretion. The invention also relates to a pharmaceutical composition comprising CLA-enriched milk fat.
WO2014063659A1 Treatment of cancer using a smad3 inhibitor The present invention resides in the discovery that Smad3, a key downstream mediator of TGF-β signaling, plays a critical role in development and progression of cancer. Thus, this application provides for a novel method of treating cancer by inhibiting Smad3 signaling, such as through administration of SIS3, an inhibitor of Smad3. Further provided are compositions and kits useful for treating cancer by way of inhibiting Smad3 signaling.
EP1453523B1 Heparin-containing ophthalmic agent The invention relates to the use of at least one pharmacologically acceptable viscosity stabilizer and at least one mucopolysaccharide having heparin activity and optionally additional pharmaceutical adjuvants for producing a pharmaceutical composition for treating dry eyes or for treating allergy-provoked irritations of the eye.
US20110177154 Tubular nanostructure targeted to cell membrane Devices, compositions, and methods are described which provide a tubular nanostructure or a composite tubular nanostructure targeted to a lipid bilayer membrane. The tubular nanostructure includes a hydrophobic surface region flanked by two hydrophilic surface regions. The tubular nanostructure is configured to interact with a lipid bilayer membrane and form a pore in the lipid bilayer membrane. The tubular nanostructure may be targeted by including at least one ligand configured to bind to one or more cognates on the lipid bilayer membrane of a target cell.
CN101972288A Powder for treating oral diseases and preparation method thereof The invention discloses powder for treating oral diseases and a preparation method thereof. The preparation method comprises the following steps of: taking 8-10 baked CoganargiopeamoenaKochs, 3g of dried alum, 6-7 incinerated silkworm cocoons, 5g of indigo naturalis and 3g of borneol and mixing and grinding the same to powder. The invention can be applied to infected parts 3-4 times per day. The infected parts can be cured within several days and the therapeutic effect is obvious.
CN103159741A Preparation and application of novel tyrosine kinase inhibitor The invention relates to a preparation and application of 2-(1H-1, 2, 3-triazole-4-group) aniline compounds, and particularly provides a 1, 4-disubstituted-1, 2, 3-triazole quinazoline compound, and the structure is shown as formula (I). The 1, 4-disubstituted-1, 2, 3-triazole quinazoline compound can be used as good tyrosine kinase inhibitor which can inhibit survival and growth of breast cancer cells BT474, SUM252, SKBR-3 and SUM190. Structure unit of R1 and structure unit of R2 are shown in the contents.
CA2264552C Method of using tetracycline compounds for inhibition of nitric oxide production The invention is a method of inhibiting the production of nitric oxide (NO) in an in vivo, in vitro, or ex vivo biological system. The method employs a tetracycline compound to inhibit the production of NO and/or to inhibit the expression or activity of an inducible isoform ot nitric oxide synthase (iNOS). Preferably, the tetraclycine compound has inhibitory activity for metalloproteinases. Also it is preferred that the tetracycline compound is provided to the biological system in an amount which has little or no antibacterial activity in the system. Accordingly, preferred tetraclycine compounds are tetracycline compounds which have been modified to reduce or eliminate their antimicrobial activity. The method can be used to treat medical conditions in mammals characterized by NO production mediated by iNOS, including, for example, inflammatory conditions.
CN102716465A Pharmaceutical composite for treating tumor and preparation method of pharmaceutical composite The invention discloses a pharmaceutical composite for treating tumor. The pharmaceutical composite is prepared from sodium cantharidinate, mannatide and auxiliary materials. The pharmaceutical composite not only can improve the immunity function of organism, but also can directly restrain and kill tumor cells, thus the pharmaceutical composite is obvious in effect and brings good news for tumor patients.
WO2012030745A1 MULTIVITAMIN TARGETING OF RNAi THERAPEUTICS Conjugates comprising vitamin B12 (Fig. 1) and oligonucleotides are useful in inhibiting expression of other oligonucelotides in a cell.
US20110059176 Material for preventing tissue adhesion and material for preventing joint contracture The present invention provides a tissue adhesion prevention material preparable at an affected area at the time of surgical procedure by producing a three-dimensional polymeric structure having a flexible structure and high solute permeability in a medium comprising water as the main component under mild conditions appropriate for body tissue components (i.e., at ordinary temperature and pressure) without conducting a chemical reaction or employing a physical procedure such as heating or light or radiation irradiation. This makes it possible to provide a tissue adhesion prevention material and a joint contracture prevention materials, which can effectively prevent postoperative adhesion of a tissue in the affected area to the surrounding tissue and contracture of the movable part of a joint. The tissue adhesion prevention material and/or the joint contracture prevention material of the present invention comprise, as the main component, a composition comprising a compound having a polyvalent hydroxyl group and a polymer containing phosphorylcholine groups and phenylboronic acid groups.
EP1660102A1 New therapeutic use of chondroitin sulphate The present invention relates to the use of an alkaline or alkaline earth metal chondroitin sulphate, which comes from an enzymatic hydrolysis of animal cartilage, for the preparation of a medicament for the treatment or prevention of psoriasis with skin affection in a mammal. Preferably the sodium chondroitin sulphate has an average molecular weight between 10,000 and 20,000 daltons, and is administered orally.
CN103648502A Pharmaceutical composition containing oleanolic acid acetate as an active ingredient for preventing or treating TLR- or IL-6-mediated diseases The present invention relates to a pharmaceutical composition for preventing or treating TLR- or IL-6-mediated diseases, containing oleanolic acid acetate or pharmaceutically acceptable salts thereof as an active ingredient, and to a pharmaceutical composition for preventing or treating TLR- or IL-6-mediated diseases and containing phaseoli semen extract, or a fraction thereof, which contains said compound or salts as an active ingredient. The phaseoli semen extract or compound according to the present invention is derived from a natural substance, which has long been used in natural medicine, and therefore causes no side effects. The phaseoli semen extract or compound inhibits the activity of TLR-3 and TLR-7 induced by Poly(I:C) and Poly(I), which are the synthetic analogues of dsRNA and ssRNA, blocks signaling pathways including NF-kappaB, and inhibits the transcriptional activity and phosphorylation of STAT3, which is an inflammation-related transcription factor activated by IL-6. Therefore, the phaseoli semen extract or compound of the present invention can be widely used in developing agents for preventing or treating TLR- and IL-6-mediated diseases, such as atopic dermatitis or arthritis.
US20120171221 Biomarkers for the early detection of autoimmune diseases Provided are methods for aiding in diagnosing autoimmune diseases in a mammal, comprising contacting a sample of tear from the mammal with an antibody that specifically binds to a first polypeptide selected from the group Ctss, Ctsh, Ctsr, Ctsw, Ctsz, Ifng, Il16ra, Il10, Il10ra, Il15, Tnfa, Apo-F, or Lcn-2 or a second polypeptide selected from the group lactoperoxidase, lactoferrin or lysozyme under conditions favoring the formation of an antibody-polypeptide complex, and determining the amount of complex formed, wherein an increased formation of antibody-first-polypeptide complex or a decreased formation of antibody-second-polypeptide complex as compared to a suitable control, indicates a likely positive diagnosis of an autoimmune disease for the mammal, thereby aiding in the diagnosis. Methods of treating the autoimmune diseases are also provided.
US20090217924 Treatment systems and methods There is disclosed a system comprising a fluid reservoir, a liquid solution within the reservoir, the solution comprising an antibiotic of the lincomycin family, a spray nozzle, a spray activator, and a tubular connection connecting the spray nozzle and the fluid reservoir.
WO2006106372A8 New crystalline atorvastatin hemicalcium salt polymorph form The present invention relates to a new crystalline polymorph B-52 form of atorvastatin hemicalcium salt [A [(3R, 5R) -7 - [3-phenyl-4 - [ (phenyl carbamoyl] -2- (4 -fluorophenyl) -5- (1-methyletliyl) -IH- pyrrole-1-yl] -3, 5-dihydroxy-heptanoic acid calcium salt (2:1)] , medicinal preparations containing the new polymorph form, process for the preparation thereof and the use of the new polymorph form for the preparation of medicinal products .
US20100087795 Self-learning drug delivery system Self-learning process for automatically adjusting a dosage of a substance administered to a person by a drug delivery device, a drug delivery device, wherein a dosage of a substance is adjusted by such a self-learning process and a drug delivery system comprising such a drug delivery device. Pain is experienced differently at certain times of day due to the origin causing the symptoms. Therefore, the medication providing pain relief should also be adjusted accordingly. The invention is to anticipate the pain experience and to deliver pain relief medication in such a way that Quality of Life is improved by appropriate timing of the right amount of medication and by appropriate timing of turning off the medication to reduce side effects.
CN101259284A Liver target anticancer nano prodrug system based on tree shaped polymer, preparation and use The invention relates to a liver targeting anticancer nanometer prodrug system basing on dendritic polymer, provides a method for preparing the prodrug system and the uses thereof and belongs to the technical field of biological medicine as well as the technical field of nano medicine. With the polyethylene glycol modified PAMAM treelike polymer of distal liver targeting group (T) as a carrier (T-PEG-PAMAM) and Doxorubicin (DOX) as treatment drug, the invention obtains the prodrug (T-PEG-PAMAM-DOX) through the covalent bond connection with degradable lysosome between the carrier and the Doxorubicin. The invention further provides the application of the liver targeting anticancer nanometer prodrug system basing on the dendritic polymer in the preparation of drugs for treating solid tumors. With the long-acting cycle in blood, the liver targeting anticancer nanometer prodrug system basing on the dendritic polymer can enhance the phagocytosis of hepatoma cells on polymers nano-micelles, realize the active and passive targeting on liver tumor tissues, improve the clinical efficacy and the bioavailability of present liver cancer therapeutic drugs and lower toxic and side effects.
CN1939293A Naprosyn alginic aid calcium gel microsphere preparation and its making method A gel micropill with low irritation to stomach is proportionally prepared from naproxen and calcium alginate through proportional mixing, adding distilled water, stirring, dropping it in the aqueous solution of CaCl2, stirring to form micropills, flushing with distilled water and drying.
CN1562023A Naloxone hydrochloride powder injection and its preparing method A powder injection of naloxone hydrochloride for dropping drug is prepared through mixing naloxone hydrochloride with the water for injection and glycine, stirring for dissolving, adding sodium hydroxide and activated carbon, stirring, adding water for injection, filter and freeze drying.
US7205317 Pain management Compounds of general formula (I) wherein R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl and triazolyl; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6 alkyl, NO2, CF3, C1–C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on thephenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, inparticular in the management of pain.
EP1059925B1 Ep2-receptor agonists as neuroprotective agents for the eye The invention relates to the use of EP2 receptor agonists as neuroprotective agents. In particular said compounds are represented by the formulae (I), (III), (IV) and (V) wherein the broken line attachment to the cyclopentane ring or the omega chain indicates the alpha configuration and the solid line attachment to the cyclopentane ring or the omega chain indicates the beta configuration, R is hydrogen or a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or -(CH2)mR1 wherein m is 0-10, and R1 is an aliphatic ring having from about 3 to about 7 carbon atoms, or an aryl or heteroaryl ring having from about 4 to about 10 carbon atoms and wherein the heteroatom is selected from the group consisting of N, O and S.
US20110244043 Controlled releasing composition A controlled releasing composition comprising a plurality of microparticles and a matrix as well as the preparation method thereof is disclosed. The plurality of microparticles comprise a first material and the matrix comprises a second material. The melting temperature of the first material is higher than the melting temperature of the second material.
US20120135929 Methods Of Modulating Uric Acid Levels Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, a compound disclosed herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
WO2009140137A9 Naphthylmethylimidizoles for the treatment of stress urinary incontinence Disclosed herein is a method of treating stress urinary incontinence comprising administering a compound to a mammal in need thereof, wherein said compound has the formula (I). Compositions and medicaments related thereto are also disclosed.
EP0781137B1 Use of phosphoglycerides comprising phosphoglycero ethers for treating neurodegenerative diseases in mentally severe handicapped children Pharmaceutical compositions relevant to the field of therapeutic chemistry and specifically to the field of phosphoglycerides are disclosed. Said pharmaceutical compositions contain phosphoglycero ethers or plasmalogens partially or predominantly combined with phospholipids derived from polyunsaturated fatty acids having 10-24 carbon atoms, and mixed or diluted with inert non-toxic carriers suitable for digestive or parenteral delivery. Said compositions may be used for treating neurodegenerative diseases.
EP1337526B1 Substituted imidazoles useful in the treatment of inflammatory diseases This invention relates to substituted imidazoles of Formula I, pharmaceutical compositons containing them, methods of using them and intermediates useful in their manufacture. The compounds of the invention modulate the production of a number of inflammatory cytokines and are useful in the treatment of diseases associated with the overpopulation of inflammatory cytokines.
WO2007135294A2 2-alkoxy-3,4,5-trihydroxy-alkylamide-benzothiazepines, the preparation and use thereof, and compositions containing the same The invention especially relates to 2-alkoxy-3,4,5-trihydroxy-alkylamide-benzothiazepines, the preparation thereof, compositions containing the same, and the use thereof as medicaments, especially anticancer drugs.
CN102309501A Novel application of artemisinin derivative The invention belongs to the field of sensitizing drugs for cancer chemotherapy, and relates to novel application of an artemisinin derivative. Specifically, the invention relates to novel application of the artemisinin derivative in preparation of a sensitizing drug for improving cisplatin chemotherapy effects. A structural formula of the artemisinin derivative is shown in the patent specification. The artemisinin derivative can be utilized for preparation of a sensitizing drug for improving cisplatin chemotherapy effects. The artemisinin derivative can improve cisplatin chemotherapy effects under the condition of low concentration, wherein under the low concentration, toxic and side effects are not produced.
EP2124950A1 Treatment of pain with naloxone A method of effectively treating nociceptive pain involves administering to a human or animal in need of relief from nociceptive pain a therapeutically effective amount of naloxone intranasally, intraveneously, by inhalation, transdermally, or orally. Pain associated with fibromyalgia, arthritis, surgical procedures, etc. can be effectively treated.
EP1419768B1 Compositions having effects of preventing or ameliorating conditions or diseases caused by brain hypofunction It is intended to provide compositions having effects of preventing or ameliorating conditions or diseases caused by brain hypofunction. These compositions contain, as the active ingredient, arachidonic acid and/or compounds having arachidonic acid as a constituting fatty acid, in particular, arachidonic acid alcohol esters, or triglycerides, phospholipids or glycolipids containing arachidonic acid as a part or all of the constituting fatty acid(s) thereof.
US20090105329 Methods of Treating Cancers with SAHA, Carboplatin, and Paclitaxel and Other Combination Therapies The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof an amount of a histone deacetylase (HDAC) inhibitor, e.g., suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and an amount of one or more anticancer agents such as Carboplatin or Paclitaxel. The HDAC inhibitor and the anticancer agents may be administered to comprise therapeutically effective amounts.
CN101352451A Anionic or cationic dendrimer antimicrobial or antiparasitic compositions The invention relates to an antimicrobial or antiparasitic composition of anion or cation dendrimer, more particularly to use of the anion or cation dendrimer in the manufacture of a medicament for inhibiting bacterial, yeast, fungus or parasitic pathogen in a human or non-human animal patient, the dendrimer has a plurality of terminal groups, wherein at least one of the terminal groups has an anionic- or cationic-moiety bonded or linked thereto, wherein the dendrimer comprises a multivalent core at least bonded covalently to the two dendritic branches, and expanded via at least two generations, and the dendrimer is polyamide amino dendrimer, polylysine dendrimer or polypropylen imine dendrimer.
EP1408943B1 Pharmaceutical formulation containing an ltb4 antagonist and a wetting agent The invention relates to a novel pharmaceutical formulation containing an LTB4 antagonist of formula (I), wherein A, R1, R2, R3 and R4 have the designation cited in claim 1. The invention also relates to the use of said formulation as a pharmaceutical.
CA2602290C Quinone derivative 2,3-dimethoxy-5-methyl-6-(10-hydroxydecyl)-1 ,4- benzoquinone for the treatment of muscular dystrophies Use of idebenone for the preparation of a medicament for the treating of a muscular dystrophy in particular for treating and/or preventing weakness and/or loss of skeletal muscle tissue and/or cardiomyopathy associated with a muscular dystrophy.
EP2257545A1 Pyrrolidinyl derivatives and uses thereof The invention relates to 3,3 disubstituted pyrrole derivatives useful for treatment of diseases associated with monoamine reuptake inhibitors.Also provided pharmaceutical compositions, methods of using, and methods of preparing the compounds.
EP1253918B1 Compositions comprising modafinil for the treatment of attention deficit hyperactivity disorder Modafinil is effective in improving symptoms of attention deficit hyperactivity disorder and symptoms of multiple sclerosis fatigue. The administration of modafinil is also shown to activate the tuberomamillary neurons of the posterior hypothalamus, and thus exhibits activity in an area of the brain associated with normal wakefulness functions. A method of identifying a compound that selectively modulates activity of the tuberomamillary nuclues of the posterior hypothalamus is also disclosed.
EP2730573A1 Methylpiperidine derivative A compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which acts relying on an orexin (OX) receptor antagonistic activity and is useful for the treatment or prevention of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, head ache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases and hypertension.
WO2011014009A3 Novel di-substituted phenoxyacetyl-based compound or pharmaceutically acceptable salt thereof, production method for same and pharmaceutical composition for suppressing multiple drug resistance comprising same as an active ingredient The present invention relates to a novel di-substituted phenoxyacetyl-based compound, a production method for the same and a pharmaceutical composition for suppressing multiple drug resistance comprising the same as an active ingredient. The novel di-substituted phenoxyacetyl-based compound of the present invention exhibits a suppressing activity on over-expression of P-glycoprotein (Pgp), which is a major cause of multiple drug resistance, and exhibits increased anticancer activity when administered conjointly with an anticancer agent such that it can be usefully employed in anticancer therapy as it can be used as a preparation for overcoming multiple drug resistance to anticancer agents, and as a therapeutic or a regulating preparation, and can enhance the effects of anticancer preparations and increase the survival rates of cancer patients, and can also lessen the side effects on normal cells since the dose(s) of the anticancer preparation(s) being used conjointly, can be reduced.
WO2013177168A1 Pyrimidine compounds for the treatment of cancer Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described.
WO2009137104A1 Combination therapy for breastcancer comprising an antiestrogenic agent This invention relates to combination therapies for the treatment of breast cancer comprising administering to a subject in need thereof a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist, or an estrogen receptor downregulator) and to compositions (e.g., pharmaceutical compositions) comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent. This invention also relates to a method of treating the side effects (e.g., vasomotor disturbances, osteoporosis and musculoskeletal complaints) associated with anti-estrogen therapy in a subject treated with one or more anti-estrogenic agents (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist or an estrogen receptor downregulator). The method comprises administering to the subject an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof.
CN101804068A Polyethylene glycol-electrolyte oral solution The invention provides polyethylene glycol-electrolyte oral solution, which comprises 59 to 60 grams of polyethylene glycol, 1.0 to 1.5 grams of sodium chloride, 0.5 to 1.0 gram of potassium chloride, 1.5 to 2.0 grams of sodium bicarbonate, 5.5 to 6.0 grams of sodium sulfate, 0.02 to 0.5 gram of edentate, 0.02 to0.5 gram of sweetener, 1 to 2 milliliters of flavoring essence and the balance of deionized water, wherein the solution is 1,000 milliliters. The polyethylene glycol-electrolyte oral solution is used in bowel cleansing and has the characteristics of quick response, safety, reliability and good cleansing effect. The oral solution is mainly suitable for cleansing bowels before colonoscopy, barium enema X-ray examination and gastrointestinal operation. The small-dose (about one eighth of a bowel cleansing dose) products of the oral solution can be used for treating chronic constipation.
US20080188492 7,8-dihydro-[1H or 2H]-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or 7,8,9-trihydro-[1H or 2H]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one, substituted at the 1 or 2 position with C2-]alkyl, C3-9 cycloalkyl, heteroarylalkyl, or arylalkyl; phosphodiesterase 1 inhibitors; Parkinsons disease The invention provides novel 7,8-dihydro-imidazo[1,2-α]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2/f]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-g allcyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.
WO2007028047A3 Immunological uses of immunodulatory compounds for vaccine and anti-infections disease therapy Methods of enhancing immune response to an immunogen in a subject are disclosed. Also disclosed are methods of reducing the sensitivity to an allergen in a subject. The methods comprise the administration of an immunomodulatory compound in specific dosing regimens that result in enhanced immune response or reduced sensitivity.
US7015213 Use of diazepines for preparing medicines for treating pathological conditions or diseases involving one of the growth hormone release inhibiting factor receptors The invention concerns the use of pyrido-thieno-triazolo-diazepins for preparing a medicine for treating pathological conditions or diseases involving one of the growth hormone release inhibiting factor receptors. The invention also concerns novel pyrido-thieno-triazolo-diazepins and therapeutic compositions containing them.
CN102920900A Compound lung-heat clearing powder and preparation method thereof The invention discloses a compound lung-heat clearing powder and a preparation method thereof. The compound lung-heat clearing powder is prepared through mixing the active pharmaceutical ingredients such as radix isatidis, semen descurainiae, venenum bufonis, bulbus fritillariae cirrhosae, pearl oyster, citrus sinensis and radix glycyrrhizae, and is prepared through eight processes such as selecting, mixing, grinding, screening, accelerated mixing, magnetic filtering, inspecting and packaging. The compound lung-heat clearing powder not only has the effects in livestock treatment of clearing away the lung-heat and relieving asthma, preventing phlegme from forming and stopping coughing, but also has obvious effects in strengthening health energy, detoxifying, preventing bacterium and diminishing inflammation from the aspects of treating the livestock lung carbuncle, acute mastitis, sore and ulcer.
US7381813 A modified estrogen receptor alpha ligand binding domain containing an amino acid modification in region 1, at region 2, or atleast one amino acid modifiation in both of regions, and these domain interacts with a nonendogenous ligand Mutants of steroid receptor ligand binding domains and synthetic ligands which have specific binding affinities for these receptors are provided. The use of these LBD-ligand combinations for construction of selective “molecular gene switches” is disclosed. Methods of regulating gene function using these switches are provided.
CA2564592C Compositions for improving breast health in women Disclosed are compositions and corresponding methods for treating fibrocystic breast disease or other breast-related disease or condition. The compositions comprise, per serving or dose, from zero to about 400 ~g selenium, from about 100 mg to about 6000 mg gamma linolenic acid, and about 0.15mg to about 5 mg iodine, with nutritional embodiments further comprising one or more of protein, fat, carbohydrate, vitamins, and minerals and providing from about 50 to about 1000 kcal of energy per severing or dose. Also disclosed are in-vitro studies showing that certain combinations of gamma linolenic acid, iodine, and/or selenium may 1) inhibit breast cancer or fibrocystic cell proliferation, 2) reinforce the function of tight junctions of endothelial cells and of mammary epithelial cells in estrogen-sensitive conditions, and 3) reduce the risk of vascular invasion by breast cancer cells.
CN101564382A Iguratimod osmotic pump controlled slow-release preparation The invention relates to a slow-release control preparation containing iguratimod and a preparation method thereof. The slow-release control preparation is an osmotic pump type double-layer tablet using osmotic pressure of an osmotic pump as main release power. The preparation consists of a double-layer tablet core, a semi-permeable membrane and a release pore, and contains high molecular materials with slow-release control function such as polyoxyethylene, cellulose acetate and the like. Compared with the common tablet, the preparation has more durable release performance and more stable blood concentration, and only needs to be taken once every day. The preparation provides better medicament selection for the treatment of rheumatoid arthritis, and reduces the risk of adverse reaction possibly caused by the fluctuation of the iguratimod blood concentration. The preparation is orally-taken slow-release control preparation, and has stable and controllable quality; and the prescription and preparation processes are reliable and feasible, and are suitable for industrialized production.
WO2014082286A1 Rafamycin analogs and methods for making same A semi-synthetic rapamycin analog with a triazole moiety or a pharmaceutically acceptable salt or prodrug thereof, is a broad-spectrum cytostatic agent and a m TOR inhibitor, and is useful in the treatment of various cancers, or tumors in organs such as kidney, liver, breast, head and neck, lung, prostate, and restenosis in coronary arteries, peripheral arteries, and arteries in the brain, immune and autoimmune diseases. Also disclosed are fungal growth-, restenosis-, post- transplant tissue rejection- and immune- and autoimmune disease- inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such triazole-moiety containing rapamycin analog is in treating renal carcinoma, lung cancer, colon cancer, and breast cancers wherein potency of the drug, its half-life, tissue distribution properties, and its pharmacokinetic properties including bioavailability through oral and intravenous routes are essential to the clinical outcomes.
CN101756923A Lovastatin and nicotinic acid double-layer sustained release tablets and preparation process The invention provides a preparation method of double-layer sustained release tablets containing nicotinic acid and Lovastatin. The combination is a double-layer tablet, wherein a nicotinic acid layer is a slow release layer, and the Lovastatin layer is a quick release layer. The invention solves the problems of different drug releasing velocity required by the nicotinic acid and Lovastatin, the nicotinic acid is prepared into the slow release layer, the Lovastatin is prepared into the quick release layer, and the two layers are pressed into the double-layer tablet. The invention solves the common problem that the double-layer tablet splits after long time setting, the prepared Lovastatin and nicotinic acid double-layer sustained release tablets not only have good appearance, but also the upper and lower layers of the tablets are tightly combined with each other; and the speed and degree of expansion of the two layers are consistent, so that the excellent appearance and the drug releasing velocity can always be maintained. The product of the invention has simple preparation method and easily available raw and auxiliary materials, is suitable for industrialized production and has excellent application prospect.
US20110020364 Methods and compositions involving pbef inhibitors for lung inflammation conditions and diseases The present invention concerns methods and compositions involving inhibitors of Pre-B Cell Colony Enhancing Factor (PBEF) for inflammatory conditions and diseases, including acute lung injury (ALI), ventilator-induced lung injury (VILI), and acute respiratory distress syndrome (ARDS). The present invention also concerns biomarkers for inflammation as well as methods for screening for PBEF inhibitors.
CN103585147A Application of Nitrosporeusines A in preparation of oral ulcer treatment or prevention medicines The invention relates to an application of Nitrosporeusines A in the preparation of oral ulcer treatment or prevention medicines for the first time. The Nitrosporeusines A has a brand new skeleton type, has a strong treatment activity against oral ulcers, has protruding substantive features, and has an obvious substantial advantage in the treatment of the oral ulcers.
WO2007036791A1 Pyrido-pyridimidine derivatives useful as antiinflammatory agents Provided are novel pyrido-pyrimidine derivatives, having the structure of Formula (I): which can be used as anti-inflammatory agents. Also provided are pharmaceutical compositions comprising one or more pyrido-pyrimidine derivatives, as well as methods of treating autoimmune diseases, inflammation or associated pathologies, including for example, sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis, comprising administering such compounds or pharmaceutical compositions comprising them.
CN1919847A Novel hydrochloride compound and use thereof The invention discloses a new anti-halo compound in the medical technological domain, which is 3-[2-(diphenyl-mesyl)-acetoxylation]-2-phenylpropionic acid9-methyl-3oxa-9-aza-tricyclic [3.3.1.02,4]-n-7-grease hydrochlorate with chemical structure formulation as formulation I modified by scopolamine structure.
CN101185632A Lonafarnib sustained-release implant for treating solid tumor A ranophanib sustained release implant for treating solid tumors is characterized in that the sustained release implant includes effective dose of anticancer ranophanib, sustained release excipients and a certain quantity of sustained release moderator. Solid tumors include lung cancer, esophageal carcinoma, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic carcinoma, bladder carcinoma and colorectal cancer. Sustained release excipients are mainly one or combination of the copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly(L-lactide-co-ethyl phosphate) and poly (L-lactide-co- phosphoric acid propyl); in the process of decompression, ranophanib can be slowly released to local tumor, thus maintaining effective drug concentration of local tumor as well as significantly reducing overall toxic reaction. Being placed in local tumor, the sustained release implant not only reduces overall toxic reaction of ranophanib, but also selectively improves drug concentration in local tumor, enhancing the therapeutic effects of non-operative therapy such as chemotherapy drugs and radiotherapy.
CN103041441A Application method of medical biocolloid liquid The invention discloses an application method of medical biocolloid liquid. According to the application method, a medical biocolloid liquid prepared in the patent with the application number of 201210267413.7 can be directly applied to an application product which is used on tissues and wounds to play effects of preventing adhesion and promoting healing, wherein 5 to 1000ml of the preparation is filled in a glass container or a plastic container, the container is capped or sealed and subjected to high-temperature moist heat sterillization to prepare the application product of the medical biocolloid liquid. The medical biocolloid liquid prepared by the method can be applied to tissues and wounds, and has the advantages of no toxicity, sensitization or stimulation to human body, and has excellent biocompatibility and degradability, so that the t-PA activity of tissues can be effectively protected, expression of PAI-1 (plasminogen activator inhibitor-1), TGF-beta1 (transforming growth factor beta 1) and TNF-alpha (tumor necrosis factor alpha) can be reduced, inflammatory exudation can be reduced, and dissolution of fibrous protein can be improved. The application product has the effects of preventing adhesion, stopping bleeding, resisting bateria, reducing exudation, and promoting tissue and wound healing.
CN103304575A Neogambogic acid derivative, preparation method thereof and pharmaceutical application The invention relates to the field of pharmaceutical chemistry and pharmacotherapeutics, and in particular relates to a neogambogic acid derivative, as well as a preparation method and a pharmaceutical application thereof. The neogambogic acid derivative has an anti-tumor function and can be used for preparing anti-tumor pharmaceuticals. The invention further relates to the preparation method of the neogambogic acid derivative.
WO2010039939A1 Janus kinase inhibitors for treatment of dry eye and other eye related diseases Methods, kits, and compositions for treating dry eye disorders and other related eye diseases are provided, wherein the methods, kits, and compositions utilize a JAK inhibitor.
CN1608626A Fosphenytoin sodium powder for injection and its prepn The present invention is fosphenytoin sodium powder for injection and its preparation, and belongs to the field of medicine technology. The fosphenytoin sodium powder for injection is prepared with fosphenytoin sodium heptahydrate in 85-90 wt%, buffering agent and pH regulator in certain proportion; and the preparation process includes the steps of dissolving fosphenytoin sodium heptahydrate in injection water, adding or adding no buffering agent, regulate pH value with sodium hydroxide and acid to 8.5-9.5, and bacteria-free freeze drying, spray drying or non-toxic organic solvent re-crystallization to prepare the powder for injection. The present invention is used in treating cramp of epilepsy patient, preventing and treating eclampsia, and has relatively high effectiveness, safety and tolerance.
CN1861050A Slow-releasing injection contg. platinum compounds and its potentiator type anticarcinogen A slow-release anticancer injection contains the slow-release microspheres and solvent. Said slow-release microsphere contains the active anticancer component chosen from 6 Pt compounds including bicycloplatinum, etc and 3 cytotoxins including phosphoinositide 3-kinase inhibitor, pyrimidine analog or DNA repairase inhibitor, and the slow-release auxiliary.
WO2010031735A1 Piperazine d3 and 5-ht2a receptor modulators The present invention relates to compounds of the general formula (I) (I) wherein X, n and R1 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, as well as their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, useful in the treatment and/or the prevention of cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and psychoses comprising paranoia and delusions.
US6894046 For treating eosinophil-dependent inflammatory diseases, asthma The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 4; X is O, S, NR5 or a direct bond; Y is O, S, NR5 or S(O)2; R1 independently is C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is Het1, C3-7cycloalkyl or optionally substituted C1-6alkyl and if X is O, S or NR5, then R2 may also represent aminocarbonyl, aminothiocarbonyl, C1-4alkylcarbonyl, C1-4alkylthiocarbonyl, arylcarbonyl, arylthiocarbonyl, Het1carbonyl or Het1thiocarbonyl; R3 and R4 independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; R3 and R4 form a C2-6alkanediyl; R5 is hydrogen or C1-4alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y—C1-4alkanediyl-C(═O)—O—R14, Het3, Het4 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl-C(═O)—O—R14, —C(═O)—O—R14, —Y—C1-4alkanediyl-C(═O)—O—R14, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R14 is hydrogen, C1-4alkyl, C3-7cycloalkyl, aminocarbonylmethylene or mono- or di(C1-4alkyl)aminocarbonylmethylene; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
CN102438623A Solid preparation containing npy y5 receptor antagonist Disclosed is a preparation which is capable of improving the water solubility of an NPY Y5 receptor antagonist even when the NPY Y5 receptor antagonist is contained in the preparation in a large amount. Specifically disclosed is a solid preparation which contains an NPY Y5 receptor antagonist, carboxymethyl ethyl cellulose, and if necessary, an amorphization inducer. The solid preparation has improved dissolvability of the NPY Y5 receptor antagonist.
EP2616441A2 Pyridine compounds and the uses thereof The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
EP2380878A1 Cyclic compound having hetero atom An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof: wherein each substituent is defined as follows: A is a 3- to 10-membered heterocyclyl group and the like, B is an amino group and the like, and X is N and the like.
EP2285812A1 HYDROGENSULFATE SALT OF 2-ACETOXY-5-(a-CYCLOPROPYLCARBONYL-2-FLUOROBENZYL)-4,5,6,7-TETRAHYDROTHIENO[3,2-c]PYRIDINE AND ITS PREPARATION The present invention relates to crystalline form I of Prasugrel hydrogensulfate. A process for the preparation of these salts, pharmaceutical compositions comprising the salts and the use of the salts as a pharmaceutical, in particular as a blood platelet aggregation inhibitor are also described. Seed crystals which can be employed in the above mentioned process as well as a process for their preparation are also disclosed.
WO2007092161A2 A direct cellular energy delivery system A lipid vesicle comprising a phospholipid which is a stable vesicle former and at least one unstable vesicle forming member, wherein the unstable vesicle forming member is selected from the group consisting of a polar lipid which is not a stable vesicle former, a PEG, a raft former and a fusion protein is provided. The vesicle can further comprise a biomolecule, such as for example ATP. Methods of using the vesicle for delivery of biomolecules are also provided.
US20080242686 Pharmaceutical compositions of lavendustin Topical pharmaceutical compositions, e.g. in form of an emulsion, comprising a lavendustin derivative of formula (I): wherein R is methyl, methoxy or ethyl, or a pharmaceutically acceptable salt thereof, and an emollient, and optionally further excipients.
US20090036528 Multifunctional and combinational application of aspartame and or futhan The present invention is an application, composition, and method of using a pharmaceutically effective amount of aspartame or its primary metabolite aspartyl-phenylalanine in systematic and periodic application or dose as an aspirin (NSAID) substitute, treatment for osteoporosis, and or topical treatment for Rosacea.
US20070059241 neutralizing monoclonal antibodies against human Insulin-like Growth Factor Receptor-I (IGFR1); anticancer agent The present invention includes fully human, neutralizing, monoclonal antibodies against human Insulin-like Growth Factor Receptor-I (IGFR1). The antibodies are useful for treating or preventing cancer in a subject. Also included are methods of using and producing the antibodies of the invention.
CN103261197A Highly-soluble pyrroloquinoline quinone salt and method for producing same The purpose of the present invention is to provide: a pyrroloquinoline quinone salt that is highly soluble in water and organic solvents; and a method for producing the pyrroloquinoline quinone salt. According to the present invention, a pyrroloquinoline quinone salt that is highly soluble in water and organic solvents, said pyrroloquinoline quinone salt comprising pyrroloquinoline quinine ions and an ammonium salt having a hydroxyl group, is provided, and a method for producing the pyrroloquinoline quinone salt is also provided.
CN102464660B 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-pyrrolizine-5-acetate-butyl nitrate crystal, and preparation method and application thereof The invention discloses a crystal of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-pyrrolizine-5-acetate-butyl nitrate. Cell parameters of the crystal are as follows: a is 14.9810(12) A, alpha is 90.00 DEG, b is 10.3310(10) A, beta is 96.272(4) DEG, c is 16.0010 A, gamma is 90.00 DEG, Z is 4, and the volume of a crystal cell is 2461.6(4) A<3>. The invention also discloses a preparation method for the crystal and application of the crystal in preparation of medicines, especially non-steroid medicines capable of relieving fever, easing pain, inhibiting arthritis and protecting gastrointestinal mucosa.
US7642378 Lipid lowering biphenylcarboxamides Biphenylcarboxamide compounds of formula (I) methods for preparing compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) as well as the use of compounds of formula (I) as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.
CN102058576A Cisplatin precursor medicine as well as preparation method thereof, and core-shell nano-particle as well as preparation method thereof The invention relates to a cisplatin precursor medicine, of which a structural formula is c,c,t-[Pt(NH3)2Cl2(O2CCH2CH2CH2CH2CH3)2]. The cisplatin precursor medicine molecule contains a -O2CCH2CH2CH2CH2CH3 group which has stronger hydrophobicity and better stability, and is easy to pack to be prepared into a nanometer dosage form of high drug load. Meanwhile, the -O2CCH2CH2CH2CH2CH3 group is easily reduced into cisplatin in an organism to act to cancer cells. In addition, the invention also relates to a preparation method of the cisplatin precursor medicine, and a core-shell nano-particle containing the same as well as a preparation method thereof.
US20120328541 Anti-radical agents Compounds of the formulae and selected hindered nitroxyl, hydroxylamine and hydroxylamine salt compounds such as the compound of the formula wherein G1 is hydrogen; C1-C22alkyl; C1-C22alkylthio; C2-C22alkylthioalkyl; C5-C7cycloalkyl; phenyl; C7-C9-phenylalkyl; or SO3M; G2 is C1-C22alkyl; C5-C7cycloalkyl; phenyl; or C7-C9-phenylalkyl; E is oxyl or hydroxyl; V is —O—; or —NH—; a is 0 or 1 or 2; b, c and d and g are each independently of one another 0 or 1; e is an integer from 1 to 4; f, m, n and p are each independently of one another an integer from 1 to 3; q is 0 or an integer from 1 to 3; Q, T and G3 are as defined in claim 1; G4 and G5 are each independently of the other hydrogen; or C1-C22alkyl; exhibit marked antiinflammatory action.
CN1559539A Medicinal mixture possessing alpha glycocidase inhibiting activity and its use A medicine with high activity to suppress alpha-glucosidase for treating diabetes, and hyperlipemia, and delaying sanility contains the common alkaloid extracted from mulberry plants and the flavone extract.
EP1414465B1 Use of inhibitors of progesterone receptor for treating steroid resistant breast cancer The invention relates to the use of progesterone receptor inhibitors for inhibition of growth-factor-dependency of tumor cells.
WO2011161687A1 Process for preparing extra pure 2, 6-diisopropyl phenol Disclosed herein is a process for the preparation of highly pure 2,6-diisopropyl phenol (Formula I), which comprises reacting p-hydroxy benzoic acid (Formula II) with an alkylating agent in presence of aq. mineral acid followed by basification and subsequent washings to yield 4-hydroxy-3,5-diisopropylbenzoic acid (Formula III) free of dimer impurity, 4, 4'-oxydibenzoic acid of Formula IV, ether impurity 3,5-di(propan-2-yl)-4- (propan-2-yloxy)benzoic acid of Formula V and the monoalkylated impurity 4-hydroxy- 3-(propan-2-yl) benzoic acid of Formula VI; and decarboxylating 4- hydroxy-3,5- diisopropylbenzoic acid (Formula III) in presence of high boiling solvent and sodium hydroxide as a catalyst at high temperature to yield 2, 6-diisopropyl phenol substantially free of ether impurity 1,3-di(propan-2-yl)-2-(propan-2-yloxy)benzene of Formula VII and monoalkylated phenol impurity 2-(propan-2-yl) phenol of Formula VIII. Propofol prepared by the process of the present invention is suitable for pharmaceutical use.
CN101857594A Tetrahydropyridoindole compounds, and preparation method and application thereof The invention discloses tetrahydropyridoindole compounds shown as formula (I) (comprising racemates, enantiomers and other stereoisomers) or pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, and also discloses a preparation method and application of the compounds, namely the compounds are inhibitors of protein kinases such as c-Met tyrosine kinase and the like, and can be used for treating diseases caused by abnormal activity of the tyrosine kinases such as tumor and the like, or can be used for preparing medicaments for treating the diseases.
EP0969836B1 Lactose-free, non-hygroscopic and anhydrous pharmaceutical compositions of descarboethoxyloratadine Stable pharmaceutical compositions of descarboethoxyloratadine (DCL), a metabolic derivative of loratadine, for the treatment of allergic rhinitis and other histamine-induced disorders are disclosed. The compositions are formulated to avoid the incompatibility between DCL and reactive excipients such as lactose and other mono- and di-saccharides. Disclosed compositions include lactose-free, non-hygroscopic and anhydrous stable pharmaceutical compositions of DCL.
CN102772503A Medicine for preventing porcine reproductive and respiratory syndrome The invention discloses a medicine for preventing porcine reproductive and respiratory syndrome (PRRS). The medicine is prepared by adding sanhuang tablets for human in a proper amount of a full value material, grinding and fully mixing to allow pigs to eat by themselves, wherein the dosage of the sanhuang tablets is as the followings according to the size of pigs: 15-40 tablets for piglets, 40-80 tablets for middle-sized piggies, 80-100 tablets for large-sized pigs, 100-150 tablets for non-pregnant sows, pregnant sows and breast-feeding sows, and each tablet is 0.44g. According to the invention, the medicine is cheap, there is no medicine residue in pigs after years of application, the medicine is quite worthy and has good prevention effect, every year pigs are allowed to take the medicine every 7-30 days one time from the beginning of summer to the beginning of winter, and pigs are allowed to take the medicine every 30-60 days one time from the beginning of winter to the beginning of summer. Experiments of four years (from 2007 to 2010) show that the epidemic prevention rate reaches 100%.
CN101953919B Alligator oil scald-burn cream and preparation method thereof The invention relates to an alligator oil scald-burn cream and a preparation method thereof, relating to a scald-burn cream and providing the alligator oil scald-burn cream having obvious effect on treating scald and burn and the preparation method thereof. The alligator oil scald-burn cream comprises the following components of 200 to 1000g of alligator oil, 1000g of vegetable oil, 60 to 150g oflithospermum, 60 to 150g of sanguisorba officinalis, 60 to 150g of astragalus root, 60 to 150g of the root of red-rooted salvia, 60 to 150g of borneol and 1000 to 3000g of albolene. The preparation method comprises the following steps of adding the vegetable oil, the lithospermum, the sanguisorba officinalis, the astragalus root, the root of red-rooted salvia and the borneol to a rotatable evaporation bottle according to the weight percentages; adding ethanol; carrying out vacuum backflow; extracting; adding the ethanol collected through the backflow to the rotatable evaporation bottle again;continuously extracting; evaporating for removing the ethanol; filtering; eliminating residues, wherein the filtrate is vegetable oil extract liquid; uniformly blending the vegetable oil extract liquid, the alligator oil and preheated albolene liquid according to the weight percentages; and cooling to prepare the alligator oil scald-burn cream.
WO2008036139A3 Inhibitors of mshc and homologs thereof, and methods of identifying same The present invention utilizes three families of bacterial enzymes, which play a key role in mycothiol biosynthesis. The three families are bacterial cysteine:glucosaminyl inositol ligases (MshC) with catalytic ligase activity for ligation of glucosaminyl inositol and cysteine, bacterial acetyl-CoA:Cys-GlcN-Ins acetyltransferases (MshD) with catalytic activity for addition of an acetyl group to Cys-GlcN-Ins and bacterial MshA glycosyltransferase with catalytic activity for production of GlcNAc-Ins. The invention provides methods for using the mycothiol biosynthesis ligases, acetyltransferases or glycosyltransferases in drug screening assays to determine compounds that inhibit activity. The invention also provides inhibitors of the production or activity of the enzymes of mycothiol biosynthesis, and use of the inhibitors for treating microbial infection.
US20120207795 Cationic polymer coated mesoporous silica nanoparticles and uses thereof A submicron structure having a silica body defining a plurality of pores is described. The submicron body may be spherical or non-spherical, and may include a cationic polymer or co-polymer on the surface of said silica body. The submicron structure may further include an oligonucleotide and be used to deliver the oligonucleotide to a cell. The submicron structure may further include a therapeutic agent and be used to deliver the therapeutic agent to a cell. An oligonucleotide and therapeutic agent may be used together. For example, when the oligonucleotide is an siRNA, the composition may be used to decrease cellular resistance to the therapeutic agent by decreasing translation of a resistance gene.
CN101416938A Slow-released injection containing nolatrexed dihydrochloride and synergist thereof The invention relates to a slow-release injection containing nolatrexed and a synergistic agent of the nolatrexed, which consists of a slow-release microballoon sphere and a solution medium, wherein, the slow-release microballoon sphere comprises active anti-cancer ingredients and slow-release accessories; and the solution medium is a special solution medium containing a suspending agent. The active anti-cancer ingredients are antimetabolites, such as pemetrexed, rumitrexed, raltitrexed, nolatrexed, carmofur, dexrazoxane, tegafur, zalcitabine, emtricitabine, ibatabine, ancitabine, decitabine, flurocitabine, enocitabine, imidazoletabine, capecitabine, gemcitabine, fludarabine or cladribine, and the like, and synergistic agents of the antimetabolites selected from topoisomerase inhibitors and/or tetrazine compounds; the slow-release accessories are selected from one of polifeprosan, di-fatty acid and decanedioic acid copolymer, polylactic acid copolymer and EVAC or the combination thereof; the viscosity of the suspending agent is 100cp to 3000cp (at the temperature of 20 DEG C to 30 DEG C) and the suspending agent is selected from carboxymethylcellulose sodium and the like. The slow-release microballoon sphere can also be prepared into a slow-release implant used for being injected or put in tumors or the surrounding of the tumors so as to enhance the effects of radiotherapy and chemotherapy.
WO2014015056A3 Anti-mucus drugs and uses therefor Disclosed are methods of identifying, generating and synthesizing compounds that inhibit MAPK13 activity. In various embodiments, compounds, salts thereof and prodrugs thereof of the present teachings can be useful for the treatment of diseases and disorders that involve excess mucus production.
WO2009084738A1 Method and pharmaceutical composition for treatment of cancer using bmp9 protein Disclosed is a therapeutic agent for cancer, which can treat solid cancer or a disease or disorder associated with the solid cancer without inducing any adverse side effect. Specifically disclosed is a pharmaceutical composition for treating and/or preventing cancer, which comprises BMP9 protein, a nucleic acid encoding BMP9 protein, an expression vector carrying a nucleic acid encoding BMP9 protein, or a combination of two or more of them as an active ingredient.
US20100151008 Preparations and Methods for Textile and or Fiber Surface Finishing, Surface Finished Articles Prepared Thereby, and Uses Therefor The invention relates to the use of liposomes, particularly liposomes based on soybean oil lecithins, for finishing textiles and fibers, a key aspect of the invention being that, besides a fiber-care effect, skin-friendly substances are transferred by liposome-finished fibers or textiles to the skin from those fibers or textiles.
CN1654039A Oral formulation of hydroxycamptothecin and its preparation method The present invention discloses one kind of oral hydroxy camptothecine preparation and its preparation process. The preparation contains hydroxy camptothecine as active component and has certain amount of alkali salt added into polyglycol as excipient to increase the digesting rate of the medicine in medium. Animal test shows that the preparation exhibits certain tumor inhibiting effect, hydroxy camptothecine dripping pill in the dosage of 8 mg/kg and 12 mg/kg has obvious experimental mouse S-180 caruncle treating effect in the action strength similar to that of hydroxy camptothecine injection, and hydroxy camptothecine dripping pill in the dosage of 4, 8 and 12 mg/kg has obvious experimental mouse Lewis lung cancer treating effect in the action strength weaker than that of hydroxy camptothecine injection in the same dosage.
WO2006064291A1 Topical formulations for use in the treatment of prevention of skin cancers Topical compositions for the treatment or prevention of skin cancers comprising a steroid selected from the group consisting of ethisterone and derivatives thereof and trilostane and derivatives thereof, the use of said steroids in the manufacture of a topical medicament for the prevention or treatment of skin cancers that can be so prevented or treated by inhibiting angiogenesis and/or vasculogenesis and a method for the treatment of prevention of a skin cancer that can be so prevented or treated by inhibiting angiogenesis and/or vasculogenesis, said method comprising the topical administration to a patient in need thereof of an effective amount of a steroid selected from said steroids.
EP2484367A1 Agent for preventing adverse side effects of carcinostatic agent The present invention provides a side effect inhibitor of drug therapy for colorectal cancer using 5-fluorouracil, comprising fucoidan or a fucoidan-containing material; a method for inhibiting side effects of drug therapy for colorectal cancer using 5-fluorouracil, which comprises administering fucoidan or a fucoidan-containing material to a colorectal cancer patient; and use of fucoidan or a fucoidan-containing material for the production of a side effect inhibitor of drug therapy for colorectal cancer using 5-fluorouracil.
WO2008079683A3 N- (5, 6, 7, 8-tetrahydronaphthalen-1-yl) urea derivatives and related compounds as trpv1 vanilloid receptor antagonists for the treatment of pain The present application is directed to compounds that are TRPV1 antagonists and have formula: (I); wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.
WO2013073763A1 Niacin-peptide having skin whitening activity and use for same Provided is niacin-peptide which has skin whitening activity. The peptide of the present invention has skin whitening activity by inhibiting melanogenesis, that is, by inhibiting the expression of a gene related to melanogenesis (for example, TRP-1, TRP2, or MIFT). The peptide of the present invention has high stability and skin permeability. Also provided is a cosmetic composition for skin whitening which contains the niacin-peptide.
US20080241212 Tyrosine-derived aromatic polyester sheet, film or mat of nanofibers optionally including anesthetics, antiinflammatories, microbiocides, leukotriene inhibitors, or antiscarring, antifibrotic, or antineoplastic agents, and that resists capsular contracture and adherence to the implant A biodegradable, flexible covering for a breast implant is provided which comprises one or more biodegradable polymer layers dimensioned and shaped to cover at least a portion of the breast implant. The implant can be inserted into an opening of the covering immediately prior to surgery, but alternate configurations and times of insertion are contemplated as well as open or sheet type devices. The coverings can optionally contain one or more drugs for delivery at the surgical site, particularly for treating or preventing infection, pain, inflammation, capsular contracture, scarring or other complications associated with breast augmentation or breast reconstruction.
CN1726920A Nose taking powder of prostaglandin E A nasally applied powder of prostaglandin E1 is disclosed.
US20090023743 Inhibitors of protein kinases Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
US20110183019 Methods of screening for and treating autism spectrum disorders and compositions for same Disclosed are methods of screening for an autism spectrum disorder, compositions that inhibit the release of molecules that disrupt the blood-brain barrier, compositions for treating autism spectrum disorders, and methods of treating autism spectrum disorders.
US20070232678 (4, 5, 6, 7-Tetrahydro-1-H-Indol-7-Yl) Acetic Acid Derivatives for Treatment of Alzheimer's Disease Compounds of formula I: are disclosed. The compounds are useful in treating or preventing diseases associated with deposition of Aβ in the brain.
EP1523239B1 Use of a composition and a cleaning tablet containing said composition for disinfecting purposes The invention relates to the use of a composition containing: - at least one organic or inorganic compound or combination of substances, which separates chlorine or bromine in an aqueous solution; and - optionally, a surfactant (tenside) or surface-active mixture of substances, aromatic substances, auxiliary agents, and binding agents. Said composition is used for disinfecting dental objects such as toothbrushes and dentures as well as shaving devices, which are infected with retroviruses, herpes viruses, pseudomonas aeruginosa, and/or candida, and body parts that are infected with retroviruses or herpes viruses, pseudomonas aeruginosa, and/or candida.
EP2190842A1 Polymorph forms of (s)-2-((4-benzofuranyl)carbonylaminomethyl)-1-((4-(2-methyl-5-(4-fluorophenyl)thiazolyl)carbonyl)piperidine New crystalline forms of (S)-2-((4-benzofuranyl)carbonylamino methyl)-1-((4-(2-methyl-5-(4-fluorophenyl))thiazolyl)carbonyl)piperidine, methods for their preparation and use in medicine as orexin receptor antagonist.
US20120172371 Fluoroquinolone derivatives or sulfonamide moiety-containing compounds as inhibitors of tyrosyl-dnaphosphodiesterase (tdp1) A method for treating cancer in a subject, comprising administering to a subject having cancer a therapeutically effective amount of (i) a fluoroquinolone derivative that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity or (ii) a sulfonamide moiety-containing compound that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity, thereby treating the cancer in the subject. In certain embodiments, the fluoroquinolone derivative or sulfonamide moiety-containing compound is co-administered with a topoisomerase I (TopI) inhibitor.
US20110160216 Thymidylate Synthase Haplotype is Associated with Tumor Recurrence in Stage II and Stage III Colon Cancer Patients The invention provides compositions and methods for determining the likelihood of tumor recurrence following treatment with 5-FU based adjuvant therapy for Stage II or Stage III colon cancer patients. After determining if a patient is less likely to experience tumor recurrence once treated, the invention also provides methods for treating these patients.
CN101390871A Ginsenoside Rb1 containing impurity ginsenoside Rd The invention discloses a standard ginsenoside Rb1 active ingredient, containing ginsenoside Rb1 with the content more than or equal to 90% and less than 100%, and impurity with the content less than or equal to 10%; the standard ginsenoside Rb1 active ingredient is also characterized in that the active ingredient contains ginsenoside Rd; wherein, the content of impurity ginsenoside Rd is more than or equal to 0.1% and less than or equal to 10%; or the content of impurity ginsenoside Rd is more than or equal to 0.5% and less than or equal to 8.0%; or the content of impurity ginsenoside Rd is more than or equal to 0.5% and less than or equal to 5.0%; or the content of impurity ginsenoside Rd is more than or equal to 0.6% and less than or equal to 3.0%; or the content of impurity ginsenoside Rd is more than or equal to 1.0% and less than or equal to 2.0%; Pharmacological experiments show that the standard active ingredient of the application has good pharmacological effects and can be prepared into pharmaceutical preparations in Pharmacy.
US8618177 Method of treating pain caused by inflammation A method of treating or inhibiting, in particular, pain caused by inflammation in a mammal by administering to the mammal an effective inflammatory pain alleviating amount of a (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound or a physiologally acceptable salt thereof, such as the hydrochloride or citrate salt.
CA2358998C Substituted bicyclic derivatives useful as anticancer agents The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3 and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals with administering the compounds of formula (1) and to pharmaceutical compositions for treating such disorders which contain the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1).
US20120178790 Crystalline form of a 3-phenoxymethylpyrrolidine compound The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
EP2177209A1 Intravenous solutions and uses The invention relates to intravenous solutions comprising a desfluoroquinolone compound for use in bacterial infections, and processes for their preparation.
US6979680 Glycosaminoglycans having an average molecular weight of 2400 D suitable for the treatment of senile dementia The present invention relates to the use of glycosaminoglycans having an average/molecular weight of 2,400 D for the preparation of pharmaceutical compositions suitable for the treatment of senile dementia, in particular for the treatment of Alzheimer's disease or SDAT (Senile Dementia Alzheimer's Type) and of the cerebral neurological lesions from ictus and from traumas.
CN103110567A Preparation method of nanometer drug delivery system carrying tanshinone IIA and application thereof The invention discloses a preparation method of a nanometer drug delivery system carrying tanshinone IIA. The preparation method comprises the following steps: step 1. preparing methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine modified by valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide; and step 2. preparing methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine nanoparticle carrying the tanshione IIA and modified by the valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide when the molar ratio of the methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine nanoparticle modified by the valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide and the tanshinone IIA is 1-60:1-60. The invention also discloses the application for the nanometer drug delivery system carrying the tanshinone IIA prepared by the method. The nanometer drug delivery system carrying the tanshinone IIA prepared by the method can effectively lower the toxicity of the tanshinone IIA and increase the targeting of the tanshinone IIA and the treatment effect.
CN103421056A Dioxane derivatives modified by glucosamine, preparation method and applications thereof The invention relates to dioxane derivatives modified by glucosamine, a preparation method and applications thereof, and specifically relates to dioxane derivatives, which are modified by glucosamine represented by the formula (I), or medically acceptable salts thereof, wherein the R1 is selected from H, benzyl, benzoyl, or alkanoyl with a carbon number of 1 to 10, the R2 is selected from H, alkyl with a carbon number of 1 to 10, alkanoyl with a carbon number of 1 to 10, aryl with a carbon number of 6 to 14, or heterocyclic radical with a carbon number of 5 to 14, the alkyl is optionally substituted by aryl with a carbon number of 6 to 14 or heterocyclic radical with a carbon number of 5 to 14. The invention also relates to a preparation method of a compound represented by the formula (I), a pharmaceutical composition containing the compound represented by the formula (I), and applications of the compound in preparing anti-inflammatory drugs.
CA2827383A1 Molecular switch for neuronal outgrowth Disclosed herein are methods of inducing neuronal outgrowth of a neuron. The methods comprise contacting the neuron with an agent that binds receptor protein tyrosine phosphatase d (RPTPd), to thereby induce neuronal outgrowth of the neuron. The agent may induces clustering of RPTPd and/or inhibit binding of chondroitin sulfate proteoglycan (CSPG) to RPTPd. Examples of suitable agents are heparan sulfate proteoglycan, heparan sulfate, heparan sulfate oligosaccharides, or heparin oligosaccharides. Additional agents are also disclosed. The neuron can be a CNS neuron or peripheral neuron. Also disclosed herein are methods of treating neuronal injury in a subject comprising, administering to the subject an agent that binds RPTPd. Administration may be to a site of neuronal injury, to thereby induce neuronal outgrowth at the site of neuronal injury.
CN102872131A Application of Houttuynoid C in anti-helicobacter pylori drug An activity experiment in vitro indicates that Houttuynoid C has strong anti-HP (Helicobacter Pylori) activity. Houttuynoid C can be used for treating diseases such as acute and chronic gastricism, gastric ulcer, duodenal ulcer and the like and applied to preparing drugs for treating acute and chronic gastricism, gastric ulcer and duodenal ulcer. The use of Houttuynoid C in preparing the anti-helicobacter pylori drug involved in the invention is disclosed for the first time; as the framework type of Houttuynoid C is a brand new framework type and Houttuynoid C has an unexpectedly high inhibition activity for the helicobacter pylori without possibility of giving any implication by other compounds, Houttuynoid C has outstanding substantive features; and simultaneously, the application of Houttuynoid C for preventing and treating the helicobacter pylori apparently has obvious progress.
CN1650870A Berberine compound sugar reducing medicine A hypoglycemic compound berberine for decreasing blood sugar, blood fat and blood viscosity and lowering blood pressure is prepared from the sulfonylurea kind of medicine and berberine.
WO2008111632A1 Glucocorticoid receptor agonist composed of 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative Disclosed is a glucocorticoid receptor agonist composed of a 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative. Also disclosed is a novel pharmacological activity of the agonist. Specifically disclosed is a glucocorticoid receptor agonist composed of a compound represented by the formula (1) below or a salt thereof. [In the formulae below, R1 represents a group represented by the general formula (2a), (3a), (4a) or (5a); R2 and R3 may be the same or different and represent a hydrogen atom, a halogen atom, a lower alkyl group or the like; R4 represents a lower alkyl group; R5, R6, R7 and R8 represent a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkoxy group or the like; and m, n, p and q represent 0, 1 or 2.]
CN102861098A Application of Houttuynoid A in medicine for preventing and treating liver injury The inventor discovers that Houttuynoid A has a prevention effect on mice acute liver injury induced by D-galactosamine (D-GalN) and has a prevention effect on mice acute liver injury induced by carbon tetrachloride (CCl4) through a pharmacological study. Therefore, Houttuynoid A can be utilized to prepare the medicines for preventing and treating liver injury or hepatitis. Application of Houttuynoid A on preparation of the medicine for preventing and treating liver injury provided by the invention is disclosed firstly. The skeleton type belongs to new skeleton type, and the activity of Houttuynoid A on the treatment effect of liver injury is unexpectedly strong; and the probability that any revelation is provided by other compounds does not exist, Houttuynoid A has the excellent substantive features, and Houttuynoid A obviously has a remarkable progress when being used for preventing liver injury.
WO2010056630A1 Triazolopyrimidinones and methods of use thereof The present invention discloses a method of treating a cardiovascular disease or condition comprising administering therapeutically effective amounts of certain triazolopyrimidinones as Fatty Acid Binding Protein ("FABP") inhibitors. Examples of such disease or condition include metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative inventive method to treat the above-noted conditions uses the administration of the compound shown below: (I)
US20130072513 COMBINATIONS OF BERBERINE, ARTEMISININ, Loperamide AND THEIR DERIVATIVES TO TREAT MALARIA, DIARRHEA, TRAVELERS' DIARRHEA, DYSENTERY, DENGUE FEVER, PARASITES, CHOLERA AND VIRUSES This invention relates to compositions and methods of combining berberine, artemisinin and loperamide or their derivatives in a therapeutic product for mammals suffering from malaria, diarrhea, travelers' diarrhea, dysentery, dengue fever, parasites, cholera and viruses by administration of a therapeutically effective amount of the composition.
US20060093575 Oxaliplatin anti-resistance agent The invention concerns a method for detecting in vitro resistance of cancer cells to an oxaliplatin treatment characterized in that it consists in measuring mitochondrial apoptosis of cancer cells being treated or capable of being treated or to be treated with oxaliplatin.
US20090191194 Inhibition of protein kinase c alpha for the treatment of cardiovascular diseases The invention relates to the use of agents impeding the expression and/or activity of protein kinase C-alpha (PKC-α), especially for treatment of patients with diabetes and complications such as diabetic nephropathy, retinopathy or neuropathy.
CA2267543C Use of sulodexide and of the medicines containing it in the treatment of the diabetic retinopathy The use of sulodexide, a glycosaminoglycan of natural origin extracted from mammalian intestinal mucosa, and of medicines containing it in the treatment of patients suffering from retinopathy of diabetic origin is the object of the present invention. The effectiveness of sulodexide has been proved by the significant lowering of the plasmatic exudation and of the hard exudates, by the improvement of the retinic lesions and by the restoration of the functional integrity of the membrane of the microcapillaries with subsequent decrease of the capillary permeability in diabetic patients treated with pharmaceutical compositions containing therapeutically effective amounts of drug.
US20100055193 Stable powder formulation containing an anticholinergic agent The invention relates to a spray-dried powder formulation comprising particles that contain the following components i) to iii): i) anticholinergic agents, in particular at least one compound of formula 1, in which X− represents a negatively charged anion, ii) at least one embedding material selected from the group consisting of mono- or disaccharides, oligosaccharides, polymers, sugar alcohols and cholesterol, iii) an organic, physiologically acceptable, sterically demanding acid, selected from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, with the exception of amino carboxylic acids, preferably fumaric acid, oxalic acid, or diacetic acid, and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, α-hydroxycaprylic acid or gluconic acid. The invention also relates to a method for producing said formulation and to the use of an organic, physiologically acceptable, sterically demanding acid from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, with the exception of amino carboxylic acids, preferably fumaric acid, oxalic acid, or diacetic acid, and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, α-hydroxycaprylic acid or gluconic acid, for stabilising a powder formulation produced by spray-drying containing the aforementioned compound of formula 1 according to i) and a suitable embedding material ii).
CN103637999A Multi-layer solid drug dosage form The invention discloses a multi-layer solid drug dosage form. A core containing an active ingredient is coated by a first layer of slow-release coating layer, and a drug layer containing an active ingredient is added, and then coated by a second layer of slow-release coating layer.
CN102973591A Application of alginic acid in preparing medicament for treating serious hepatitis The invention discloses novel application of alginic acid in preparing a medicament for treating serious hepatitis. The medicament can be used for inhibiting inflammatory reaction in serious hepatitis attaching process, so that attack or symptom worsening of serious hepatitis can be inhibited. Alginic acid has good curative effect in an endotoxin and D-galactosamine induced animal model; and the medicaments used in the application can be easily acquired, low in price and stable in properties, are convenient to store and transport, and have wide application prospect.
EP1877044A2 N-acetylcysteine amide (nac amide) for the treatment of diseases and conditions associated with oxidative stress Methods and compositions comprising N-acetylcysteine amide (NAC amide) and derivatives thereof are used in treatments and therapies for human and non-human mammalian diseases, disorders, conditions and pathologies. Pharmaceutically or physiologically acceptable compositions of NAC amide or derivatives thereof are administered alone, or in combination with other suitable agents, to reduce, prevent, or counteract oxidative stress and free radical oxidant formation and overproduction in cells and tissues, as well as to provide a new source of glutathione.
US7041696 Induce inflammation, immunology response; autoimmune disease; antiarthritic agents The present invention relates to interleukin-1β converting enzyme inhibitors having the formula: R is a carbocyclic or heterocyclic ring; R1 is a cysteine trap; R2a, R2a′, R2b, and R2b′ are each independently hydrogen, C1–C4 alkyl, C1–C4 alkoxy, and mixtures thereof; or R2a′ and R2b′ can taken together to form a double bond; L and L1 are linking groups having the formula: T is selected from the group consisting of: i) —NR6—; ii) —O—; iii) —NR6S(O)2—; iv) —S(O)2NR6—; and v) mixtures thereof; R6 is hydrogen, substituted or unsubstituted C1–C20 linear, branched, or cyclic alkyl, C6–C20 aryl, C7–C20 alkylenearyl, and mixtures thereof; the indices w, w1, and w2 are each independently 0 or 1; i) hydrogen; ii) C1–C4 linear, branched, and cyclic alkyl; iii) R3a and R3b or R4a, and R4b can be taken together to form a carbonyl unit; iv) two R3a or two R3b units from adjacent carbon atoms or two R4a or two R4b units from adjacent carbon atoms can be taken together to form a double bond; and v) mixtures thereof; the index m is from 0 to 5; the index n is from 0 to 5.
CN1887292A Soft lentinan capsule and its prepn The present invention discloses one kind of soft lentinan capsule and its preparation process, and the soft lentinan capsule is prepared through suspending lentinan in diluent to form stable suspension and filling the suspension into soft capsule shell. Of each 1000 capsules in 334.45-824.07 g, there are lentinan 10-50 g, diluent 100-400 g, gelatin 50-180 g and glycerin 14.1-64.5 g. The inclusion contains lentinan, diluent and suspending agent; and the capsule shell contains gelatin, glycerin, water, preservative and antioxidant. The soft lentinan capsule has the functions of benefiting Qi, invigorating spleen, tonifying deficiency and strengthening body's resistance, and may be used in treating chronic hepatitis B and as the assisting medicine for radiotherapy and chemotherapy treating tumor in digestive tract. The present invention has the advantages of stable quality, convenient taking and high bioavailability.
CN103385516A Liquid supplement The invention relates to a liquid supplement. The liquid supplement comprises the following raw materials: conjugated linoleic acid, tea polyphenol, vitamin E, ubiquinone, pantothenic acid, vitamin A and isoflavone. According to the further technical scheme, the raw material contents of the liquid supplement are as follows: the conjugated linoleic acid is 1 to 4 g/kg, the tea polyphenol is 200 to 500 mg/kg, the vitamin E is 5 to 100 mg/kg, the ubiquinone is 1 to 2 mg/kg, the pantothenic acid is 4 to 7 mg/kg, the vitamin A is 5 to 100 mg/kg and the isoflavone is 50 to 200 mg/kg. The liquid supplement used for conditioning a human body through the combined action of the raw materials, so that the skin is ruddy, fine, smooth and glossy, and is improved fundamentally.
WO2007020388A1 Pyrazole derivatives as therapeutic agents Salts of 1,5-diarylpyrazole-3-carboxamides and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
CA2524300C Modified-release tablet of bupropion hydrochloride A modified-release tablet of bupropion hydrochloride comprising (i) a core comprising an effective amount of bupropion hydrochloride, a binder, a lubricant; and (ii) a control releasing coat surrounding said core; and (iii) a moisture barrier surrounding said control releasing coat, wherein the modified-release tablet is bioequivalent to Wellbutrin© or Zyban®/Wellbutrin®SR tablets.
CN101935274A Process for producing medicinal zinc citrate The invention provides a process for producing medicinal zinc citrate and belongs to the field of pharmaceutical chemicals. In the process, the weight ratio of citric acid (based on anhydride) to zinc oxide is 1:0.65-0.70; and the product zinc citrate is prepared by reacting solution of citric acid with zinc oxide suspension with the granularity of below 180 meshes at the initial temperature of between 38 and 40 DEG C, filtering, clarifying, filtering, rinsing and drying. The purity of the medicinal zinc citrate produced by the process is over 99 percent and the yield is over 87 percent.
CN101239123A Medicaments for treating renal failure The present invention relates to a medicine for treating renal failure, which is characterized in that the medicine consists of raw materials as follows: 5-100 parts by weight of snakegourd, 50-1000 parts by weight of wick, 20-1500 parts by weight of red fushen, 10-100 parts by weight of shanzhizi, 10-100 parts by weight of white peony, 10-100 parts by weight of angelica. The medicine has the effect of treating renal failure, saving renal with calculous, through sanjiao, changing to precious, separating qing and zhuo, removing blood stasis and restoring deficiency syndrome, diminishing inflammation and discharging fire, clearing away damp-heat, eliminating feeling of repletion, conducing relieving oneself, removing tibial medium pain, regulating yin-yang, cleaning source etc. The medicine has the obvious curative effect in treating bladder heat accumulate, gonorrhoea atresia, liquid channel atresia, astringent heat pain, and is used for removing smear, bean juice, residual urine, red acerbity, white urine, blood urine and pain, heat hematochezia, renal failure, sanjiao arthralgia due to stagnation of qi and nephritis etc.
US7785811 Using lutetium label probes to detect tumor secreted antigens and diagnose/prognose cell proliferative disorders Described is a novel gene and its encoded secreted tumor antigen, termed BPC-1, and to diagnostic and therapeutic methods and compositions useful in the management of various cancers which express BPC-1, particularly including prostate cancer and bladder cancer. In human normal tissues, BPC-1 is only expressed in certain tissues of the brain. However, BPC-1 is expressed at high levels in prostate cancer cells and is also expressed in bladder cancer cells. The structure of BPC-1 includes a signal sequence and a CUB domain. BPC-1 protein is secreted. Preliminary experimental evidence suggests that BPC-1 is directly involved in oncogenesis or maintenance of the transformed phenotype of cancer cells expressing BPC-1. BPC-1 also appears to bind specifically to a cellular protein expressed in prostate cancer cells and other cells.
CA2283829C 2-alkylidene-19-nor-vitamin d compounds The invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula (I) where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 and R8, which may be the same or different, are each selected from hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or when taken together represent the group -(CH2)x- where x is an integer from 2 to 5, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by low intestinal calcium transport activity and high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover osteoporosis.These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.
WO2002099074A3 Slc7s as modifiers of the p53 pathway and methods of use Human SLC7 genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of SLC7 are provided.
US20090203028 Novel aptamers that bind to listeria surface proteins Aptamers bind to Listeria surface proteins. A method of assaying a sample for the presence of Listeria monocytogenes includes exposing the sample to an aptamer that specifically binds one of the following proteins: Listeria monocytogenes internalin A protein, Listeria monocytogenes internalin E protein, and Listeria monocytogenes 0610 protein. The presence of Listeria monocytogenes in the sample is detected when the aptamer binds the protein present in the sample. A method of treating Listeria monocytogenes infection includes administering the aptamers to the mammal at a concentration sufficient to reduce Listeria monocytogenes infection.
CN102786461A Arbidol hydrochloride crystal E, its preparation method and its applications in medicines and healthcare products The invention discloses an Arbidol hydrochloride crystal E substance with the structure represented by formula (I), a preparation method of an Arbidol hydrochloride crystal E sample, products prepared through treating the Arbidol hydrochloride crystal E substance as an active component, and applications of the Arbidol hydrochloride crystal E in the disease control and the healthcare, wherein the products comprise medicines and healthcare products.
US7833999 histamine H3 receptor modulators; obesity, diabetes and central nervous system diseases such as vigilance and sleep disorders; e.g. (+)-2-(cyclohexylmethyl)-N-[2-(1-methylpyrrolidin-2-yl)ethyl] -1,2,3 ,4-tetrahydroisoquinoline-7-sulfonamide The invention relates to tetrahydroisoquinoline sulfonamide compounds (of formula (1) as defined in the specification), their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.
WO2010121576A3 Novel 7-deazapurine nucleosides for therapeutic uses The invention provides compounds of formula I, wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds and/or compositions. ˙
CN102988331A Use of 2-mercapto-3-butanol in preparation of anti-lenticular opacity products The invention relates to a new use of 2-mercapto-3-butanol and a composition thereof in the treatment of lenticular opacity. The efficacy of the 2-mercapto-3-butanol in the aspects of preventing and treating the lenticular opacity and the like is mainly as follows: the anti-lenticular opacity action is realized by closing a channel which is positioned between nonessential mercapto of crystallin and profilin and can form a disulfide bond for causing nonspecific accumulation and further contain the formation of the macromolecular crystallin, a new medicament source and an application formulation are provided for the chemical control of cataract, and the important reference value is further realized for preventing and treating other age-related eye diseases. The 2-mercapto-3-butanol disclosed by the invention has the advantages of safety, low price, significant efficacy and stable nature, is suitable for large-scale production and commercial application in medicines, reagents and other industries and easy to popularize and apply, and further has good application prospects and significant social benefits and economic benefits.
CA2757723A1 Method of predicting a predisposition to qt prolongation based on abcc2 gene sequence or product thereof The present invention describes an association between genetic polymorphisms in the ABCC2 gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval-prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation.
CN1606979A Effect of scutellarein as antifebrile, analgesic, antiphlogistic, antibiotic and antiviral agent Said invention relates to scutellarin. The scutellarin and its salts accepted in medical use are used in preparing refrigerating, pain easing, anti-inflammation, anti-biotic and antiviral medicine for treating fever, headache, throat sore, myalgia, arthralgia, infection of respiratory and pneumonia, having good cure and prevention effect.
CN101389607A Substituted arylsulfonamides as antiviral agents The invention relates to substituted arylsulfonamides of formula (I) and to processes for preparing them, to their use for producing medicaments for the treatment and/or prophylaxis of diseases, particularly for use as antiviral agents, especially against cytomegaloviruses.
US7229996 For therapy and prophylaxis of infectious diseases in mammals, both humans and non-humans, having antibacterial activity against drug-resistant bacteria Novel rifamycin derivatives of formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or their salts, hydrates or prodrugs thereof, wherein: a preferred R comprises hydrogen, acetyl; L is a linker, a preferred linker group elements selected from any combination of 1 to 5 groups shown FIG. 1, provided L is not wherein R1 is H, methyl or alkyl. The inventive compounds exhibit valuable antibiotic properties. Formulations having these compounds can be used in the control or prevention of infectious diseases in mammals, both humans and non-humans. In particular, the compounds exhibit a pronounced antibacterial activity, even against multiresistant strains of microbes.
WO2005030765A1 Quinazoline derivatives as antiproliferative agents The invention concerns quinazoline derivatives of Formula (I), wherein each of R1a, R1b, R2, R3 and a have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.
CN102388812A Beef cattle nose ring The invention discloses a beef cattle nose ring and belongs to the field of apparatuses for livestock. The beef cattle nose ring comprises an annular nose ring. The nose ring comprises a left half ring and a right half ring. One ends of the two half rings are hinged together and the other ends of the two half rings are respectively detachable fastener structures. The beef cattle nose ring is characterized in that the surface of at least one half ring is provided with a row of depressed pits and solid medicines are filled into the pits; and the solid medicines are mixtures of bingpeng powder and vitamin K, and the mass ratio of the bingpeng powder to the vitamin K is (3-5):1. After the bingpeng powder and the vitamin K are evenly mixed, the mixtures are wrapped by gauze and are filled intothe pits, the solid medicines in the gauze gradually seep when the gauze rubs with a beef cattle nose, and the effects of continuously stopping bleeding, clearing heat, removing toxic substances, eliminating swelling, relieving pain, promoting rapid wound healing and preventing infection on the beef cattle nose are taken.
EP1628533A2 Chemokine receptor binding heterocyclic compounds with enhanced efficacy The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infections of target cells by a human immunodeficiency virus (HIV).
US20100158918 Polypeptides and polynucleotides encoding same The invention provides polypeptides, designated herein as SECP polypeptides, as well as polynucleotides encoding SECP polypeptides, and antibodies that immunospecifically-bind to SECP polypeptide or polynucleotide, or derivatives, variants, mutants, or fragments thereof. The invention additionally provides methods in which the SECP polypeptide, polynucleotide, and antibody are used in the detection, prevention, and treatment of a broad range of pathological states.
WO2014037343A1 Composition for treating psoriasis A dermal composition for treating or soothing psoriasis lesions, wherein the composition comprises a tar extract, a corticosteroid, an antipruritic, an antibiotic, urea, an absorption base, water, lanolin, and propylene glycol.
CN102114009A Pharmaceutical composition containing tomoxetine and preparation method thereof The invention relates to a pharmaceutical composition containing tomoxetine and a preparation method thereof. The pharmaceutical composition contains tomoxetine and carrier auxiliary materials which are pharmaceutically acceptable, and the pharmaceutical composition can exist in solid or liquid form, wherein the essential ingredient is added by being dispersed in a solution.
CA2359541C Anticonvulsant derivatives useful in treating cluster headaches The use of anticonvulsant derivatives of formula (I) treating cluster headaches is disclosed. Wherein X is CH2 or oxygen; R1 is hydrogen of C1-C4 alkyl; and R2, R3, R4 and R5 are independently hydrogen or C1-C3 alkyl and, when X is CH2, R4 and R5 may be alkene groups joined to form a benzene ring and, when X is oxygen, R2 and R3 and/or R4 and R5 together may be a methylenedioxy group of the following formula (II): wherein R6 and R7 are the same or different and are hydrogen, C1-c~3 alkyl or R6 and R7 together with the carbon to which they are attached are joined to form a cyclopentyl or cyclohexyl ring.
CN103372041A Component with anticoagulation and preparation method thereof The invention relates to a component with anticoagulation and a preparation method thereof. The extract is prepared by the method as follows: extracting pseudo-ginseng or ginseng or American ginseng twice by 70% methanol, and decompressing and concentrating the extraction liquid till the extraction liquid is dry to obtain a component A; dissolving the component A, passing macroporous resin by a dissolving liquid, sequentially eluting by water, 20%, 30%, 40% and 50% ethanol to respectively collecting 30% and 50% eluants; and respectively decompressing and concentrating till the extraction liquid is dry to prepare components B and C, wherein anticoagulation of the component C is remarkably superior to that of the component B.
US20060287372 Pharmaceutical preparations containing thiazolidinediones showing new therapeutic indications The present invention refers to new therapeutic applications of pharmaceutical formulations containing, as active principles, thiazolidinediones.
US20100280013 Carbinol derivatives having heterocyclic linker [Object] It is to provide a novel LXRβ agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C═O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.)
WO2008061428A1 The pharmaceutical formulations, use and preparation of triacontanol Disclosed are the use of triacontanol in the production of medicines for treating hyperlipidemia, the pharmaceutical formulations containing triacontanol and the preparation method of triacontanol. Said formulations are consisted of pharmaceutically active agents, controlled release component and immediate release component, having the following weight ratios: triacontanol 90-110, ethyl cellulose 50-70, Eudragit II 10-30 and starch 50-70. Said preparation method is carried out as following steps: (1) using the whole plant crude powder of Euphorbiaceae Euphorbia as raw material, which being heat reflux extracted with ethanol, methanol or acetone, and then concentrating the extract; (2) degreasing the concentrate produced in step (1) to obtain solids; (3) subjecting said solids to silica gel chromatogramphy, collecting eluants, recovering solvents and crystallizing the obtained solid with ethyl acetate to give flaky crystal.
US20060264418 6-(2,2,2-Trifluoroethylamino-7-chloro-2,3,4,5-tetrahydro-1h-benzo[d] azephine as a 5-ht2c receptor agonist The present invention provides a 7-chloro-6-(2,2,2-trifluoroethylamino)-2,3,4,5-tetrahydro-1H-benzo[d]azepine of formula (I): or a pharmaceutically acceptable salt thereof, and its use as a selective 5-HT2c agonist for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, anxiety, and depression.
CN101019953A Medicine for treating bronchitis and asthma The present invention is one kind of medicine for treating bronchitis and asthma. The medicine is prepared through mixing Langdu root powder in 0.05-0.1 weight portions; fine medicine powder prepared with chinarue 30-50 wt%, astragalus root 20 -30 % and Shantugua 30-40 wt% and through water extraction and other steps in 0.5-1 weight portions and theophylline powder in 0.1-0.3 powder. The medicine of the present invention has high curative effect, short treating period and less recurrence.
US7304043 β-L-2′-deoxy-nucleosides for the treatment of hepatitis B This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-eythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro pentofuranonucleoside or in combination with another anti-hepatitis B agent.
US7521455 Histamine H3 receptor antagonist or inverse agonist activity; metabolic diseases, circulatory diseases, or nervous system diseases; e.g. 3-(4-((1-cyclobutyl-4-piperidinyl)oxy)phenyl)-2-ethylpyrido(2,3-d)pyrimidin-4(3H)-one The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).]
CN101220359B SiRNA sequence restraining bak gene expression The invention relates to a siRNA double-strand sequence, which is a siRNA sequence for inhibiting bak gene expression. The invention solves the problem that the prior art has no siRNA sequence which is most appropriate for inhibiting the bak gene expression, the sequence is siRNA1: an antisense strand is 5'-AGUGCACACUUGCUAAAGCtt-3' and a sense strand is 5'-GCUUUAGCAAGUGUGCACUtt-3'; the siRNA double-strand sequence which is provided by the invention can be used for preparing drugs for inhibiting neural cell apoptosis or treating neurodegenerative diseases. The siRNA double-strand sequence enters into a biosome in a certain mode, which is the specific expression for inhibiting disease-related proteins and is more effective than any means; the invention can lead related disease genes to be in silence, carry out effective knockout to the expression of a target gene and achieve treatment purpose, and the specificity of the sequence and the powerful effect of the gene inhibition effect are unbeatable compared with the other drugs.
CN101766593A Medical composition containing amorphous atorvastatin calcium The invention discloses a medical composition containing amorphous atorvastatin calcium and a preparation method thereof. By adopting the medical composition, the stability of the medicines is obviously improved, the disintegration speed fastened and the dissolution improved. The medical composition is used for treating high cholesterin lipidemia, can reduce administration dosage, avoids great quantity of medication, enables the blood drug concentration of patients to be smooth and simultaneously increases compliance.
US20110160277 Modulation of 11 beta-hydroxysteriod dehydrogenase 1 expression for the treatment of ocular diseases The invention relates to siNA compositions and methods for the treatment of eye conditions wherein the siNA compound capable of inhibiting the expression of 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD1).
US20130004506 Method for treating pathologies associated with hypoxia using mif inhibitors Methods are provided for treating pathologies associated with hypoxia with an MIF inhibitor. Methods are also provided for treating a subject having, or at risk for pulmonary hypertension, with an MIF inhibitor. Methods are also provided for treating a subject having, or at risk from, a CNS disorder associated with hypoxia, with an MIF inhibitor. Methods are also provided of treating severe chronic lung disease, hypoxia-induced right ventricular hypertrophy or hypoxia-induced pulmonary vascular remodeling with an MIF inhibitor. Methods of diagnosing a subject with pulmonary hypertension are also provided.
US20100055048 Acute treatment of headache with phenothiazine antipsychotics Methods of treating headache with antipsychotics are provided. A kit for treating headache is also provided, comprising an antipsychotic and a device for rapid delivery of the antipsychotic.
CN103169707A New medical application of lauric acid monoglyceride The invention requests protection of application of lauric acid monoglyceride for preparing a medicine for treating or preventing diabetes and a medicinal composition containing lauric acid monoglyceride for treating or preventing the diabetes, and belongs to the field of medicines. When lauric acid monoglyceride is used for treating the diabetes, the blood sugar reduction effect of lauric acid monoglyceride is superior to that of the existing blood sugar reduction medicine pionlitazone; lauric acid monoglyceride can be used together with the existing blood sugar reduction medicine; because of combination of lauric acid monoglyceride and pionlitazone, synergistic effects on reduction of the blood sugar level, the urine sugar level and the glycosylated hemoglobin level are realized; and based on the combination of lauric acid monoglyceride and pionlitazone, rosuvastatin is added, so that the blood lipid level and the blood sugar level of diabetes patients can be further reduced. Lauric acid monoglyceride and the medicament composition containing lauric acid monoglyceride are precise in curative effect, low in side effects and low in cardiovascular risks in treatment of diabetes, thereby having good medical application prospect.
WO2011062864A3 Inhibitors of nox enzymes and methods of use thereof Inhibitors of Nox enzymes, such as Noxl, Nox2, and Nox3, and methods of making and using such compounds are describe herein.
US6919332 Enzyme inhibitors such as 5-(2-Methoxy-ethyl)-5-(4-(1-pyridin -3-yl-1H-indazol-5-yloxy)-phenoxy)-pyrimidine-2,4,6-trione, used as antiinflammatory and anticarcinogenic agents The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
EP2752413A1 Quinazoline derivative and application thereof This invention provides a class of quinazoline compounds, as represented by formula (I), and their pharmaceutically acceptable salts, wherein: each of R1 and R2 independently, is selected from H, C1-C6 alkoxy, halo-C1-C6 alkoxy, C1-C6-alkoxy-C1-C6 alkoxy, C3-C8 cycloalkoxy, C3-C8 heterocycloalkoxy containing at least one of heteroatoms selected from N, O, S; Z is -NR4-, C(R5)2, S or -O-, wherein R4 is H or C1-C3 alkyl, R5 is the same or different, selected from H or C1-C3 alkyl; R3 is selected from H, halogen, C1-C6 alkyl, C1-C6 alkoxy or halo-C1-C6 alkyl; n is an integer from 0 to 5. This invention also provides methods of preparation and medical uses of the compounds of formula (I) and their pharmaceutically acceptable salts. These compounds have the activity of inhibiting EGFR-TK, and can be used as drugs for the treatment of protein tyrosine kinase related diseases such as tumours, cancers, etc.
CN1660124A Application of gentiopicrin in preparing medication for restraining hepatitis B virus An application of gentiopicroside in preparing the medicine with it in conjunction of pharmacologically acceptable carrier for suppressing HBV is disclosed. It may be tablet, capsule, powder, pill, particle, or injection.
EP2279193A1 Novel triazole derivatives, their preparation and their application in therapeutics The present invention relates to novel compounds of formula (A): in the form of a free base or of an addition salt with an acid. The invention also relates to process of preparation of compounds of formula (A), to composition comprising them and to their application in therapeutics and in particular in cancers.
US20080058263 Polypeptides that binds to cellular receptors; animal growth regukators The present invention provides polypeptides that bind cellular receptors for vascular endothelial growth factor polypeptides; polynucleotides encoding such polypeptides; compositions comprising the polypeptides and polynucleotides; and methods and uses involving the foregoing. Some polypeptides of the invention exhibit unique receptor binding profiles compared to known, naturally occurring vascular endothelial growth factors.
CN103012537A Dammarane type triterpene compound and preparation method and application thereof The invention relates to a dammarane type triterpene glycoside compound obtained by extracting and separating from tetraploid gynostemma pentaphyllum, and a preparation method and application of the dammarane type triterpene glycoside compound. The compound, and optical isomers, medicinal salt derivatives and solvates of the compound have a purpose of preparing an anti-inflammatory drug, can be applied in self-forms, and can also be applied by forming drug compositions with acceptable carriers in pharmacy; the preparation method is simple and easy to operate; and the obtained compound is high in purity, and has a good economic benefit and an industrial application prospect.
WO2009074990A3 Rtp801l sirna compounds and methods of use thereof The invention provides chemically modified siRNA oligonucleotides that target RTP801L, compositions comprising same and to the use of such molecules to treat, inter alia, respiratory diseases including acute and chronic pulmonary disorders, eye diseases including glaucoma and ION, microvascular disorders, angiogenesis- and apoptosis-related conditions, and hearing impairments
CA2402191C Use of insulin for the treatment of cartilagenous disorders The present invention relates to methods for the treatment and repair of cartilage, including cartilage damaged by injury or cartilagenous disorders, including arthritis, comprising the administration of insulin and/or insulin variants. Optionally, the administration may be in combination with a cartilage agent (e.g., peptide growth factor, catabolism antagonist, osteo-, synovial, anti-inflammatory factor), in an extended- or sustained-release form. Alternatively, the method provides for the treatment and repair of cartilage damaged by injury or cartilagenous disorders comprising the administration of insulin and/or insulin in combination with standard surgical techniques. Alternatively, the method provides for the treatment and repair of cartilage damaged by injury or cartilagenous disorders comprising the administration of chondrocytes previously treated with an effective amount of insulin and/or insulin variant.
WO2012034116A2 Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders The invention provides for novel compounds which are inhibitors of lysine- specific demethylase 1 (LSDl). Such compounds may be used to treat disorders, including cancer.
CN101011407B Amphotericin B liposome antigungal eye drops and its preparation method The invention relates to a method for preparing amphotericin B liposome antimycotics eye drops, wherein, said eye drops is formed by antimycotics compositie drug as amphotericin B, liposome phosphatide and sterol, liposome propping agent sugar, and water/buffer. The eye drops have significant antimycotics function. And the external test has proved that its indexes can reach homogeneous chemical drugs, but higher integrated treatment effect. And the inventive drug has clear mechanism of action, and related consumption and effect. Compared with present technique, the inventive eye drops have advanced controllable quality and treatment effect.
CN103599096A Resveratrol tablet The invention discloses a resveratrol tablet, which is mainly prepared from resveratrol, soy isoflavone, calcium and vitamin D as main raw materials.
WO2012147597A1 Camptocormia therapeutic agent The present invention addresses the problem of treating camptocormia related to the external abdominal oblique muscle. This problem can be solved by administering a local anesthetic to the external abdominal oblique muscle.
CA2613350A1 Glycolipid derivative and drug containing the same as active component A glycolipid derivative represented by the formula (I): (I) wherein R1 represents an aldopyranaose residue, R2 represents a hydrogen atom or a hydroxyl group, A represents -CH2-,-CH(OH)-CH2- or -CH=CHCH2-, Z represents -O-or -CH2-, and y represents an integer of 26 to 35 when Z represents -O- and x represents an integer of 4 to 16, y represents an integer of 0 to 35 when Z represents -O- and x represents an integer of 17 to 25, y represents an integer of 26 to 35 when Z represents -CH2- and x represents an integer of 4 to 15 and y represents an integer of 0 to 35 when Z represents -CH2- and x represents an integer of 16 to 25; and a therapeutic agent for an autoimmune disease (e.g., autoimmune arthritis), an allergic disease (e.g., bronchial asthma) or a disease of which an NKT cell or the stimulation of an NKT cell is known to be involved in the aggravation of the condition comprising the glycolipid derivative.
USRE41425 Piperazine and piperidine compounds A group of new piperazine and piperidine compounds having interesting advantageous pharmacological properties and have the formula (a) wherein A represents a heterocyclic group having 5-7 ring atoms wherein 1-3 heteroatoms selected from the group O, N and S are present, R1 is hydrogen or fluoro, R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2, Z represents carbon or nitrogen, and the dotted line represents a single bond when Z is nitrogen, and represents a single or double bond when Z is carbon, R3 and R4 independently are hydrogen or C1-4-alkyl, n has the value 1 or 2, R5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R6)q, Y is a phenyl, furanyl or thienyl group, which groups may be substituted with 1-3 substituents from the group hydroxy, halogen, CF3, C1-4-alkoxy, C1-4-alkyl, cyano aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl, R6 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3 and salts thereof, are disclosed.
WO2008059518A3 Process for preparing crystalline aripiprazole The present invention relates the process for preparation of stable polymorph of aripiprazole and in particular the present invention is related to an improved process for the preparation of crystalline anhydrous aripiprazole and its hydrochloride salt.
US20090004232 Bioactive pharmaceutical/cosmetic compositions and mixed solubilization process for the formulation thereof Physically stable pharmaceutical/cosmetic compositions contain at least one hydrophilic phase, at least one lipophilic phase and at least one active principle, e.g., at least one steroidal anti-inflammatory agent, anti-fungal agent, anti-parasitic agent, nuclear receptor modulator and/or sex steroid, said at least one active principle being present in dissolved state in each of these phases; these are formulated via characteristic multi-step methodology.
CN101028511A Oral-cavity disinfectant An oral disinfecting liquid is prepared from ammonium bidecalkyldimethyl chloride, polyhexamethylene guanidine, and bilogic enzyme through heating dissolving, mixing and cooling. Its advantages are high effect, broad spectrum, and no poison and pollution.
CN102603689A Norditerpenoid compound Lachnin A, and preparation method and application thereof The invention relates to the technical field of medicines, and particularly relates to a norditerpenoid compound Lachnin A separated from a marine animal sponge, and a preparation method and application thereof. The preparation method comprises the following steps: extracting the sponge with ethanol by conventional percolation, concentrating, and purifying by separation to obtain the Lachnin A, of which the molecular formula is C19H30O3. The invention has the advantages of simple preparation technique, high yield, stale property, stable preparation quality and low production cost, can easily control the quality and is convenient for industrial production; the compound can be used for resisting inflammations, tumors, diabetes and obesity, has the advantages of obvious curative effect, high safety, low toxicity, multiple functions and abundant and cheap raw material sources, is convenient to use, and provides a new medicine source and safe raw material for preventing, diagnosing, detecting, protecting, treating and researching tumors, diabetes and obesity as wells as directly correlated diseases.
US20120115927 Pharmaceutical agent for preventing cell death Disclosed is a pharmaceutical agent for preventing cell death. The occurrence of cell death can be prevented by inhibiting the function of Int6 protein in an affected area. Then, a pharmaceutical agent comprising a substance capable of inhibiting the function of Int6 protein is prepared. The pharmaceutical agent can be used for preventing cell death.
CN103735563A Pharmaceutical composition for treating fatty liver and application of pharmaceutical composition The invention belongs to the technical field of a medicine, and particularly relates to a pharmaceutical composition for treating a fatty liver and application of the pharmaceutical composition. The pharmaceutical composition comprises the following raw materials: friedeli-3beta-alcohol, an astragalus membranaceus polysaccharide component A2, a lycium barbarum polysaccharide component VI, ajugol A and phillyrin. The pharmaceutical composition has the advantages of significant effect and stable quality control, and is applicable to long-term taking of a sufferer, and the fatty liver can be effectively treated.
CN101322805A Plaster for activating blood, resolving stasis, dispelling arthralgia spasm and easing pain, and preparation The invention discloses a plaster for activating blood circulation, dissipating blood stasis, dispelling arthralgia and easing pain and a preparation method thereof. The plaster is prepared by the steps of immersing musk, rhubarb, amber, frankincense, myrrh, Chinese angelica, pangolin scales, dipsacus root, pleione rhizome, red peony root, dahurian angelica root, blood of dragon, rhizome of drynaria, wild ginger root, gamboge, herb of diverse wormwood, saffron, notoginseng, Sichuan pepper, anisetree bark, rhizome of Chinese paris, gastrodia tuber, hornet nest, minium, menthol, triperygium wilfordii and calomel into oil according to certain proportion, decocting and cooling, etc. The plaster has no side and toxic effect, has good curative effect on diseases such as rheumatic waist and leg joint pain and swelling, bone and muscle pain caused by hyperosteogeny, female dysmenorrheal, etc. In addition, the plaster has the advantages of high curative effect, short course of treatment and quick action.
US20050148626 Novel thromodulin expression promoters It is intended to provide a novel pharmaceutical effect of HMG-CoA reductase inhibitors, in particular, (+)-(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dihydroxy-6-heptenoic acid or its salt. Namely, TM expression promoters, more specifically speaking, antithrombotic drugs, preventive/remedies for sepsis, antiplatelet drugs and anticoagulants comprising as the active ingredient an HMG-CoA reductase inhibitor, in particular, (+)-(3R, 5S, 6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dihydroxy-6-heptenoic acid or its salt.
CN1768760A Medicinal composition containing safflower total flavone and its preparation process and usage The invention discloses a medicinal composition containing total safflower flavones for treating cardiac and cerebral vascular diseases, which comprises total safflower flavones and aceglutamide by a predetermined proportion.
CN102895314A Medicine with weight-reducing and lipid-lowering functions The invention discloses a medicine with weight-reducing and lipid-lowering functions. The medicine is prepared from, by weight, 5-20 parts of a gordon euryale seed water extraction product, 4-8 parts of red monas rice, and 3-6 parts of allitricin. The medicine provided by the invention has substantial weight-reducing and lipid-lowering functions, and causes low toxic and side effects and low adverse reactions. The medicine is safe and reliable, and has potential to be developed into novel weight-reducing and lipid-lowering medicines.
US20080139522 Re-epithelializing pharmaceutical compositions comprising xanthan gum The present invention relates to the use of xanthan gum as re-epithelializing agent and, in particular, to a pharmaceutical formulation comprising xanthan gum as a re-epithelializing active principle eventually mixed with hyaluronic acid. Said use and composition speed up and improve advantageously the formation of newly grown epithelium.
WO2013121214A1 Reduction of gastrointestinal tract colonisation by campylobacter Campylobacterare the commonest reported bacterial causes of gastroenteritis in the UK and industrialized world. This invention relates to a method of preventing or reducing the colonisation of the gastrointestinal tract of an animal with Campylobacter. Accordingly, the present invention provides a method for disinfection of an animal comprising administering to said animal at least one compound that binds to MOMP or FlaA of Campylobacter in an effective amount to reduce the number of Campylobacter present in the gastrointestinal tract of said animal. The present invention also provides a method for preventing or reducing transmission of Campylobacter infection from one animal to another.
CN102816251A High-activity astragalus polysaccharide and preparation method of pharmaceutical composition of high-activity astragalus polysaccharide The invention discloses a preparation method of high-activity astragalus polysaccharide. Further, the invention relates to an astragalus polysaccharide containing pharmaceutical composition prepared from the astragalus polysaccharide. A preparation method of the astragalus polysaccharide comprises the following steps of: crushing Radix Astragali medicinal material, immersing it into a CaO aqueous solution, and successively carrying out ultrasonic extraction, cryoprecipitation, centrifugation, microfiltration, ultrafiltration, reverse osmosis and spray drying to obtain the astragalus polysaccharide. The extracted astragalus polysaccharide provided by the invention has high activity and high yield. In addition, the preparation method has a simple technology, is time-saving, energy-saving, highly efficient and simple, and is easy for popularization, development and application.
WO2012047265A2 Improved adjuvant system for vaccine administration The present invention provides adjuvant compositions that have improved stability, increased potency and which provide an enhanced Th,1 response. The present invention also provides methods of making those compositions and administration of the improved adjuvant compositions
EP2588112A2 Methods and compositions for treatment of multiple sclerosis Methods and formulations for the treatment of multiple sclerosis with drugs with affinity for both serotonergic 5-HT2 and dopaminergic receptors such as the D2 receptor are herein disclosed. According to one embodiment, a method includes delivering a therapeutic dosage of drugs with affinity for both serotonergic 5-HT2 and dopaminergic receptors such as the D2 receptors to a subject exhibiting symptoms of multiple sclerosis to alleviate the symptoms.
CN101040893A Blueberry capsule for protecting vision and the preparing method Disclosed is a vision protection capsule containing blueberry, which is prepared from the following raw materials (by weight ratio): blueberry extract 6-10, beta-carotene 10-15, vitamin B1 0-2, vitamin B2 0-2, vitamin B6 0-3, vitamin C 0-5, nicotinic acid 0-0.3 and balancing starch.
EP2651931A1 Fused dihydropyrans as gpr119 modulators for the treatment of diabetes, obesity and related diseases The present invention relates to compounds of general formula (I), wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
CN101058595A Ibonucleic acid, and preparation method and application thereof The invention discloses a method for making and using sameribonucleic acid, which comprises the following steps: adding the water homogenate to a fresh pancreas; mixing the homogenate liquor with the saturated phenol homogeneously; bruising the cells exhaustively; changing the protein nature; centrifugalizing the aqueous phase; extracting the aqueous solution with the chloroform; centrifugalizing the aqueous phase; adding the alcohol to the aqueous phase in order to precipitate the sameribonucleic acid. The invention extracts the sameribonucleic acid effectively in the cow's pancreatic, which lasts the short time for production; improves the volume of production; reduces the environment pollution; guarantees the safety.
US7008627 dermocosmetic blends useful for improving and treating hyperreactive skin conditions, allergic-type reactions and/or intolerance; anti-radical, anti-inflammatory and anti-allergenic; immunomodulatory activity This invention relates to new dermocosmetic and pharmaceutical compositions which are useful for improving and treating hyperreactive skin conditions and more generally allergic-type reactions and/or intolerance phenomena, whether they are caused by external factors or factors intrinsic to the individual. The compositions of this invention preferably contain an anti-radical, in anti-inflammatory and an anti-allergic activity for the treatment of sensitive and/or allergic skin.
US20120014934 Enhanced Natural Colors A natural color is concentrated to intensify color range and to provide useful amounts of one or more of anti-oxidant, nutritional, and anti-inflammatory compounds derived from one or more pigment sources. In a preferred embodiment, the pigment source is a fruit, a vegetable, a legume, a spice, algae, or a combination thereof.
CN103690481A Application of methane injection in preparation of medicaments for treating ischemia-reperfusion injury The invention discloses an application of methane injection in preparation of medicaments for treating ischemia-reperfusion injury, which comprises a preparation method of the methane injection. Animal experiments are performed on the methane injection, and the results prove that the methane injection can be used for obviously reducing the level of alanine transaminase, reducing liver injury and reducing hepatocyte apoptosis against a rat model with liver ischemia-reperfusion injury, so that the methane injection can be used for treating the liver ischemia-reperfusion injury. Thus, the methane injection disclosed by the invention can be used for preparing the medicaments for treating the ischemia-reperfusion injury.
WO2010055526A1 A novel polymorph of emtricitabine and a process for preparing of the same A polymorph of emtricitabine, wherein said polymorph displays angular positions of characteristic peaks in powder X-ray diffraction pattern 13.61± 0.2, 15.54± 0.2, 19.49± 0.2, 20.55± 0.2, 25.89± 0.2, 28.09± 0.2 and 29.10± 0.2. A pharmaceutical composition comprising a polymorph of emtricitabine displaying angular positions of characteristic peaks in powder X-ray diffraction pattern 13.61± 0.2, 15.54± 0.2, 19.49± 0.2, 20.55± 0.2, 25.89± 0.2, 28.09± 0.2 and 29.10± 0.2. A process for the preparation of a polymorph of emtricitabine comprising the steps of (a) dissolving crude emtricitabine in polar organic solvent by heating at a temperature of at least 40°C and not more than 150°C to form a reaction mixture optionally decreasing the concentration of polar organic solvent in said reaction mixture; cooling the reaction mixture obtained in step (a); and separating the solid from the cooled reaction mixture resulted in step (b).
WO2014067473A1 N-(5-(quinolin-6-yl)pyridin-3-yl) benzsulfamide derivatives, preparation method and therapeutic use thereof The present invention relates to the field of medical technology, and in particular, to a variety of substituted N-(5-(quinolin-6-yl)pyridin-3-yl)benzsulfamide derivatives represented by formula (1) (groups therein are as defined in the specification). The compounds according to the present invention have favorable anti-tumor activity against human lung cancer, colon cancer, liver cancer, breast cancer and glioblastoma multiforme, which contribute to development of highly effective, low toxic and high specific anti-tumor drugs, and have high value of development. The present invention also relates to a composition, preparation method and use thereof in the preparation of anti-tumor drugs.
US20080311217 Topicial composition for treating pain Topical compositions having as the active ingredient a lipid, fatty acid ester, natural wax, sterol, or combinations thereof referred to herein as “lipophilic vehicle” or “LV” and methods of use, have been developed for the amelioration or prevention of pain or the sequelae of pain. The composition may be in the form of an ointment, cream, gel, lotion, spray, foam, paste, patch, suspension or dispersion. In the preferred embodiment, the formulation is a gel. The LV may contain a penetration enhancer, most preferably one with membrane disruptive properties. The formulation may be applied to or impregnated into a gauze, wrap, bandage, cotton-tipped stick, adhesive bandage strip, or other support wrap or medical bandage or wound cover. For example, the compositions may be are incorporated onto or into disposables such as hemorrhoid wipes, sponge, mouth guards, dental trays; needles or catheters; adult diapers; gloves, socks or wrist bands, for ease of application. The composition is applied topically to a site at or adjacent to a painful region. The composition is reapplied as necessary. Pain relief is typically obtained within minutes and lasts for periods of variable duration ranging from minutes to several hours and even, in some cases, days. The composition is variably effective to treat visceral, somatic and neuropathic pain both acute and chronic as well as muscle pain and stiffness and joint pain and stiffness.
US20100261724 Heterocycle phenyl amide t-type calcium channel antagonists The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
US20110046599 Multi-Day Delivery Of Biologically Active Substances Compositions and methods for modifying biologically active substances to achieve multi-day delivery of such substances, particularly through oral or parenteral administration, are disclosed. The compositions include the biologically active substance conjugated to a carrier having a suitably long half life, typically more than one day, wherein the conjugate optionally contains a spacer linking the carrier to the biologically active substance. Pharmaceutical formulations of the conjugates are also disclosed, as are methods of extending delivery of a single dose of a biologically active substance for more than one day.
CN102198143A Application of harpagoside in pharmacy The invention develops new applications of harpagoside in medical treatment and health care, and exploits a new application area. The invention approves that oral administration of harpagoside has an obvious protective action on degenerative change of nigrostriatal dopaminergic neurons of the central nervous system, and such protective action comprises two aspects of prevention and treatment; theinvention also approves that the harpagoside is closely related to the improvement of the gene expression and protein levels of glial cell line-derived neurotrophic factor (GDNF), thereby solving theproblem that although the GDNF has actions on preventing and treating the degenerative change of the nigrostriatal dopaminergic neurons, the GDNF can not pass through the blood brain barrier; and theinvention approves that the harpagoside has good application prospects in treating or preventing neurodegenerative diseases, especially Parkinson's disease.
EP0698108B2 Adenoviral vectors of animal origin and use thereof in gene therapy Use of a recombinant adenovirus of animal origin containing a heterologuous DNA sequence for the preparation of a pharmaceutical composition for use in the therapeutic and/or surgical treatment of the human body.
CN102988345A Application of Aphanamixoid A for preparing human fungal resistant medicine The invention relates to application of Aphanamixoid A for preparing a human fungal resistant medicine, belonging to the field of medicines. Aphanamixoid A has strong effects on inhibiting trichophyton rubrum, microsporum lanosum or trichophyton tonsurans, therefore, Aphanamixoid A can be used as a human fungal resistant compound and is hopeful to be used for preparing related medicines. The application of Aphanamixoid A for preparing the human fungal resistant medicine is disclosed for the first time; because the skeleton type belongs to a brand new skeleton type and the human fungal inhibitory activity of Aphanamixoid A is strong unexpectedly, the possibility that other compounds give any inspiration does not exist; Aphanamixoid A has outstanding substantive characteristics; and simultaneously, Aphanamixoid A has obvious progress for preventing and treating human fungal infection.
EP2588113A1 A reconstituted high density lipoprotein formulation and production method thereof A reconstituted high density lipoprotein formulation having relatively low toxicity comprises an apolipoprotein such as ApoAI or fragment thereof, a lipid and a detergent at a level which is about 5-50% of that which would normally cause liver toxicity upon administration to a human. The lipid is optimally phosphatidylcholine at about 30-50g/L and the molar ratio of apolipoprotein:lipid is optimally in the range 1:40 to 1:75. The formulation is useful for treating diseases or conditions such as cardiovascular disease, hypercholesterolaemia and hypocholesterolaemia inclusive of acute coronary syndrome (ACS), atherosclerosis and myocardial infarction.
US20080033036 Composition and Method for Promoting Hair Growth The present invention provides a method and composition for promoting hair growth in a mammal which comprises a prostaglandin compound having two hetero atoms at the 15 position as an active ingredient thereof.
US20100212033 Novel ubiquitin lifases as therapeutic tragets The present invention relates to the discovery, identification and characterization of nucleotides that encode novel substrate-targeting subunits of ubiquitin ligases. The invention encompasses nucleotides encoding novel substrate-targeting subunits of ubiquitin ligases: FBP1, FBP2, FBP3, FBP4, FBP5, FBP6, FBP7, FBP8, FBP9, FBP10, FBP11, FBP12, FBP13, FBP14, FBP15, FBP16, FBP17, FBP18, FBP19, FBP20, FBP21, FBP22, FBP23, FBP24, and FBP25, transgenic mice, knock-out mice, host cell expression systems and proteins encoded by the nucleotides of the present invention. The present invention relates to screening assays that use the novel substrate-targeting subunits to identify potential therapeutic agents such as small molecules, compounds or derivatives and analogues of the novel ubiquitin ligases which modulate activity of the novel ubiquitin ligases for the treatment of proliferative and differentiative disorders, such as cancer, major opportunistic infections, immune disorders, certain cardiovascular diseases, and inflammatory disorders. The invention further encompasses therapeutic protocols and pharmaceutical compositions designed to target ubiquitin ligases and their substrates for the treatment of proliferative disorders.
US20080249124 Conjugate linkage is removable upon administration; 41-Desmethoxyrapamycin-L-wortmannin; antineoplastic agents An anti-neoplastic wortmannin conjugate is described formed by a linking a rapalog and wortmannin. Such a linkage is removable following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.
US20080153851 Cycloalkyl Piperidine Tachykinin Receptor Antagonists The present invention is directed to certain piperidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
CN102060683A Lentinus striguellus compound as well as preparation method and application thereof The invention relates to a Lentinus striguellus compound as well as a preparation method and application thereof. The preparation method comprises the following steps: culturing Lentinus striguellus strains; performing crude extraction; and refining to prepare the Lentinus striguellus compound which is colorless and oily and has antitumor activity.
WO2014100665A1 1,4-pyridone bicyclic heteroaryl compounds The present invention relates to 1,4-pyridone bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
CN103450371A Tetrahydro-beta-carbolinyl-3-formacyl-diethylenetriamino-beta-cyclodextrins, and preparation, antithrombotic activity and application thereof The invention discloses 6-[(1,2,3,4-tetrahydro-beta-carbolinyl-3)-formacyl-diethylenetriamino]-6-desoxy-beta-cyclodextrins prepared by connecting tetrahydro-beta-carbolinylcarboxylic acid to cyclodextrins by using diethylenetriamine as a connecting arm and a preparation method thereof. The invention further discloses favorable in-vivo antithrombotic activity of the compounds. The invention provides excellent candidate compounds for developing medicines with high bioavailability and strong antithrombotic activity.
WO2009102193A1 A composition comprising bifidobacterium infantis and fructo- and galacto-oligosaccharides for the prevention of intestinal discomfort in infants Compositions comprising bifidobacteria and galactooligosaccharides and fructooligosaccharides are provided that support the introduction of solid weaning foods in the diet of infants that receive infant milk formula or breast milk.
CN1823818A Medicine formula for treating finea pedis A medicine for treating beriberi contains proportionally liquor, white vinegar, sodium hydroxide and edible salt.
WO2011094431A1 Sustained-release nsaid/hmg coa reductase inhibitor compositions Compositions for controlled release of one or more therapeutic agents where the composition is essentially free of excipients are disclosed. In particular, compositions comprising a HMG-CoA reductase inhibitor, particularly simvastatin, and a NSAID, such as a COX-2 inhibitor, particularly celecoxib, in which greater than 90% of the weight of the composition is made up of the HMG-CoA reductase inhibitor and NSAID are provided.
CN101830916A Cefbuperazone sodium hydrate, preparation method thereof and application thereof The invention relates to a cefbuperazone sodium hydrate, a preparation method thereof and application thereof. The cefbuperazone sodium hydrate has high storage stability, and is suitable to be used in the preparation of medicaments for treating and preventing diseases, caused by Gram-positive or negative bacterial sensitive bacteria, such as diseases in respiratory systems, liver and gall systems and five sense organs of human beings or animals, urinary tract infection, enterocoelia infection, pelvic cavity infection, ichorrhemia, skin and soft tissue infection, bone and joint infection and the like.
US20050059735 Cyclic amino acid derivatives useful as pharmaceutical agents Pro-drug compounds of the formula (I) or (II) and compositions containing them are provided that when administered to humans or other mammals provide an increased duration of active compound in the plasma compared to compounds of corresponding structure in which labile groups are not present. In the above formulae n, P, Q, R1, R2 and R3 are as defined in the specification. The compounds may be used to treat a range of neurological conditions, e.g. epilepsy or pain.
US20060234344 Protein kinases The present invention relates to novel kinase polypetides, nucleotide sequences encoding the novel kinase polypetides, as well as various products and methods useful for the diagnosis and treatment of various kinase-related disease and conditions.
US20090275603 NF- kB Inhibitors And Uses Thereof A new class of imidazolines as 4-position esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma, etc.), antibacterial agents, and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-κB as well as potent activity against the Gram (+) bacterium. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.
CN1568994A Targeted freeze dried nanometer powder injection of hydroxycamptothecine bean phospholipid and its preparation and usage The invention discloses a targeted freeze dried nanometer powder injection of hydroxycamptothecine bean phospholipid and its preparation and usage, wherein the powder injection comprises active raw material hydroxycamptothecine, bean phospholipids as carrier, surface active agent and cryodesiccation auxiliary materials.
CN103483322A 5-fluoro-1H-benzimidazole-4-formamide derivatives, as well as preparation method and medical application thereof The invention relates to the field of medicinal chemistry, and particularly relates to 5-fluoro-1H-benzimidazole-4-formamide derivatives, as well as a preparation method and medical application thereof. A pharmacodynamic test proves that the antitumor effect of the compound disclosed by the invention can be improved by combined application with other cytotoxic antitumor drugs; meanwhile, the toxicity of the existing antitumor drug is reduced.
CN102232923A Low-dose Tenofovir compound by injection delivery and application thereof The invention relates to a low-dose Tenofovir salt-containing preparation by injection delivery, and also to a preparation method of Tenofovir salt, a preparation method of the preparation by injection delivery and an application of the preparation in the prevention and treatment of viral hepatitis B or human immunodeficiency virus infection. The preparation provided by the invention is characterized in that it is prepared by the mixing of single-dose Tenofovir salt and auxiliary materials with Tenofovir being 2mg-100mg and has advantages of lower dosage, higher biological availability and lower toxicity.
US20080045584 Use of Docetaxel for Treating Hepatocellular Carcinoma The present invention is based on the finding that docetaxel is significantly more active against hepatocellular carcinoma cells than paclitaxel at concentrations of up to 1 μM. It accordingly provides the use of docetaxel, or a hydrate thereof, in the manufacture of a medicament for use in the treatment of hepatocellular carcinoma.
CN103172627A Heterocyclic benzopyrimidine or quinoline compound and applications thereof The invention discloses a heterocyclic benzopyrimidine or quinoline compound and an application of the heterocyclic benzopyrimidine or quinoline compound. The invention further discloses a synthesizing method of the compound in formula I, pharmaceutically acceptable acid, salt or stereoisomer of the compound, and applications of the compound and the pharmaceutically acceptable salt or stereoisomer thereof in medicines for treating or preventing tumor, wherein all the groups are described in the specifications in detail. The compound is not influenced by Gleevec and can be used for effectively solving a drug-resistant problem of the Gleevec. I.
WO2011147588A1 Compositions for use in genetic disorders comprising 4-phenyl- butyric acid and its salts The present invention refers to pharmaceutical compositions comprising the histone hyperacetylating agent phenyl-butyric acid or a physiologically acceptable salt thereof for use in the treatment of a genetic disorder, especially of an epigenetic disorder, like treatment of antisocial personality disorder, depression, vaginitis and varicosis or the prevention of Sudden Infant Death Syndrome with a genetic disorder background.
EP2350012A2 Quinoline compounds as inhibitors of angiogenesis, human methionine aminopeptidase, and sirt1, and methods of treating disorders Described herein are methods of inhibiting methionine aminopeptidase or SirT1, inhibiting angiogenesis, and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, SirT1 and/or angiogenesis, wherein a compound of the invention is administered to a subject.
WO2008035177A3 Combination of mt1 and mt2 melatonin receptor agonists and a norepinephrine/dopamine reuptake inhibitor The present invention relates to the use of a combination of a MTl and MT2 melatonin receptor agonists and a norepinephrine/dopamine reuptake inhibitor (NDRI) for the treatment of depression and other affective disorders. It specifically relates to the use of a combination of agomelatine and bupropion for the treatment of depression and other affective disorders.
US20130023558 CARBOXYLIC ACID DERIVATIVES HAVING AN OXAZOLO[4,5-c]PYRIDINE RING Carboxylic acid derivatives having an oxazolo[4,5-c]pyridine ring The invention therefore relates to compounds of the formula I in which X, Y, R1, R2 and R3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.
US20120245125 Pyridazine compounds, compositions and methods The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for, research, drug screening, and therapeutic applications.
US7109291 Compounds capable of modulating the activity and stimulating the production of a catalytic antibody The invention concerns novel compounds capable of modulating the activity and stimulating the production of catalytic antibodies. More particularly, the invention concerns a compound capable of increasing the activity of an antibody having specific affinity for the catalytic site of the antibody, and it is not immunogenic. Such compounds are useful in particular for therapeutic treatment or prevention of a pathology related to an enzymatic deficiency, to stimulate in vivo hydrolysis of xenobiotics, drugs, medicines or any other molecule potentially toxic for the organism or for preventing or inhibiting allergic reactions.
US20070258970 Methods for Inhibiting Hiv and Other Viral Infections by Modulating Ceramide Metabolism The present invention provides methods of preventing infection by retroviruses and methods of treatment of patients suffering from or susceptible to a viral infection. More particularly, the present invention provides methods of preventing viral infection and methods of treating retroviral infections which comprise the administration of at least one compound comprising N-4-(hydroxyphenyl)retinamide. Preferred methods of the invention are suitable for use in the treatment of patients who are HIV positive or are suffering from or are susceptible to AIDS.
US20100166887 DIBENZO[b,e][1,4]DIAZEPINE MODULATORS OF DOPAMINE RECEPTORS, SEROTONIN RECEPTORS, ADRENERGIC RECEPTORS, ACETYLCHOLINE RECEPTORS, AND/OR HISTAMINE RECEPTORS The present invention relates to new dibenzo[b,e][1,4]diazepine modulators of dopamine receptors, serotonin receptors, adrenergic receptors, acetylcholine receptors, and/or histamine receptors, pharmaceutical compositions thereof, and methods of use thereof.
US20110165100 Compositions comprising avermectin/azelaic acid compounds useful for treating, e.g., rosacea Pharmaceutical/dermatological compositions useful for the prevention/treatment of disorders of the skin, especially rosacea, contain thus effective amounts of at least one avermectin compound, e.g., ivermectin, and at least one azelaic acid compound or salt or derivative thereof, formulated into a physiologically acceptable medium therefor.
EP2152719A1 Bicyclic heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis. Formula (I).
US6956060 Use of R-enantiomer of N-propargyl-1-aminoindan, salts, and compositions thereof The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an effective illness, a neurodegenerative disease, a neurotoxic injury, stroke, brain ischemia, a head trauma injury, a spinal trauma injury, neurotrauma, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject. Finally, the subject invention provides methods of preparing R(+)-N-propargyl-1-aminoindan, a salt thereof, and racemic N-propargyl-1-aminoindan.
CN101347422B Uses of salvianolic acid A in preventing and/or treating diabetes and complication The invention discloses a salvianolic acid A which can reduce blood sugar of animals, promote cellular glucose absorption, alleviate diabetic hyperglycemia, prevent and treat diabetic cardiovascular complications, diabetic nephrosis, diabetic peripheral circulatory disorder and diabetic peripheral nervous lesion, decrease blood lipid, reduce weight of mammals and improve generation of a cellular energy substance ATP so as to promote wound healing and metabolism function, thus the salvianolic acid A can be used for preventing and treating the diabetic hyperglycemia, the diabetic cardiovascular complications, the diabetic nephrosis, the diabetic peripheral nervous lesion, the peripheral circulatory disorder (angiopathy, diabetic gangrene and foot ulcer), obesity and hyperlipemia, can promote wound healing (various wounds, burn, scald, cutaneous erosion, decubitus as well as skin injury and mucosal injury caused by skin grafting and radiation).
WO2011151359A1 Combined treatment with a cholinesterase inhibitor and a thiadiazolidinedione derivative A combination of a cholinesterase inhibitor and a thiadiazolidinedione derivative; a pharmaceutical composition comprising a cholinesterase inhibitor and a thiadiazolidinedione derivative; a medical kit useful for administering in combination a cholinesterase inhibitor and a thiadiazolidinedione derivative; a method or treatment with a combination of a cholinesterase inhibitor and a thiadiazolidinedione derivative.
US20110165065 Means for the detection and treatment of prostate cells The present invention relates to a composition for the detection and the treatment of prostate cells and to methods for the diagnostic and therapeutic treatment of a human being using the composition according to the invention.
CN1813709A Safflower yellow dropping pill, and its preparing method and use The present invention provides a carthamus yellow dripping pills preparation. It contains carthamus yellow and at least one matrix selected from polyethylene glycol, gelatin, stearic acid, polyvinylpyrrolidone and glyceryl monostearate. The weight ratio of the carthamus yellow and the described matrix is 1-10:20-40. Said carthamus yellow dripping pills can be used for preventing and curing angiocardiopathy and cerebrovascular disease.
US20110086831 Procalcitonin for the diagnosis of bacterial infections and guidance of antibiotic treatment in patients with acute stroke or transient ischemic attack The present invention relates to an in vitro method for the diagnosis and treatment guidance of a bacterial infection in patients suffering from an acute ischemic or hemorrhagic stroke, comprising the determination of the level of Procalcitonin (PCT) or a fragment thereof having at least 12 amino acid residues in a sample of a bodily fluid from said patient and the correlation of the determined level to the diagnosis of a bacterial infection in said patient.
CN103720648A Injection containing mepivacaine hydrochloride and preparation method thereof The invention belongs to the technical field of medicine preparation, and in particular relates to an injection containing mepivacaine hydrochloride and a preparation method thereof. The method comprises the following steps: (1) boiling injection water according to the prescribed amount, cooling to 55-65 DEG C, adding mepivacaine hydrochloride and medical auxiliaries according to the prescribed amount into 20-80 percentage by weight of the injection water, stirring until the materials are completely dissolved to prepare a liquid medicine; (2) adding medical activated carbon into the liquid medicine, stirring and adsorbing at 45-55 DEG C for 10-60 minutes, decarburizing and filtering; (3) adding the rest injection water into the filtrate, regulating the pH value of the liquid medicine to 5.0-6.0 with alkali liquor, and uniformly stirring and mixing; (4) filtering, sampling, inspecting whether the product is qualified or not, filling, sterilizing at 121 DEG C for 10 minutes, and packaging. Compared with the prior art, the injection is simple in preparation process and high in stability, and can be uniformly released in a body to reduce the side effect.
US7276504 Nasally administering an imidazotriazinone substituted with an (alkoxy)(aminosulfonyl)phenyl group for treating diseases including psoriasis, female infertility, diabetes, glaucoma, cystic fibrosis, pre-eclampsia, Parkinsonism, tinnitus, pain, gastric motility disorders, and pulmonary hypertension The present invention relates to the use of known 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position and cGMP PDE-inhibitory properties for the production of medicaments for the treatment of cardiac insufficiency, psoriasis, female infertility, cancer, diabetes, ophthalmic disorders such as glaucoma, disorders of gastric motility, cystic fibrosis, premature labour, pulmonary hypertension, bladder disorders, prostate hyperplasia, nitrate-induced tolerance, pre-eclampsia, alopecia, Parkinson's disease, pain, tinnitus or the renal syndrome.
WO2014072380A1 Use of nad and ss-nad as a bronchodilator The molecule NAD and the diastereomer thereof ß-NAD have a muscle-relaxant effect on the musculature of the airways, particularly on the bronchial musculature. Therefore NAD and the diastereomer thereof ß-NAD open up a new approach for the therapy and prophylaxis of a number of diseases, disorders and conditions in which the concentration of free calcium in the muscle cells of the airway musculature is abnormally changed. Consequently, a suitable pharmaceutical preparation with the active ingredient NAD or the diastereomer thereof ß-NAD is provided as a medicine against diseases which are accompanied by a constriction of the airway musculature.
EP1442133B1 Use of Mirtazapine for improving the therapeutic response of humans having major depression and carrying the gene for apolipoprotein E4 This invention relates to methods for improving the treatment of major depression in a human patient by genotyping the patient for the gene for apolipoprotein E4 and adapting the further treatment of the patient accordingly depending on the presence or absence of the gene in the patient. The invention also relates to methods for improving the therapeutic response of human patients with major depression by determining the apolipoprotein E genotype of a human patient and administering a noradrenergic transmission enhancing anti-depressant drug, such as mirtazapine, in an amount effective to treat major depression, to those patients who are found to carry the gene for apolipoprotein E4. Also disclosed are methods for improving the therapeutic response of a human patient with major depression comprising administering mirtazapine, in an amount effective to treat major depression, to a human patient who is a carrier of the gene for apolipoprotein E4.
US7531651 e.g. 4-({[({[(2S)-4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}amino)carbonyl]amino}methyl)benzamide benzenesulfonate dihydrate; chemokine (C-C motif) receptor antagonist; antiinflammatory agent; asthma, rhinitis Compounds of formula (I): wherein A− represents the benzenesulphonate (besylate) anion;. R represents H or C1-6 alkyl; and n is a number from 0.8 to 2.2 are CCR3 antagonists and are therefore indicated to be useful in therapy are described.
US20120220631 USE OF 5H-THIOENO(3,4-c)PYRROLE-4,6-DIONE DERIVATIVES AS TUMOR NECROSIS FACTOR INHIBITOR A method of treating or curing a disease caused by or associated with elevated levels of TNF in a patient including administering to the patient 5H-thioeno(3,4-c)pyrrole-4,6-dione derivatives.
CN102846573A Silibinin double-layer slow-release tablets and preparation method thereof The present invention discloses silibinin double-layer slow-release tablets, which comprise an immediate release layer and a slow-release layer, wherein the immediate release layer mainly comprise a silibinin solid dispersion, a filler, a disintegrating agent and a lubricant, the slow-release layer mainly comprises silibinin, a slow-release material, a filler, a lubricant and a binder, a weight ratio of the silibinin content in the immediate release layer to the silibinin content in the slow-release layer is 2:8-3:7, and a weight ratio of the immediate release layer to the slow-release layer is (1.5-2.4):1. A purpose of the present invention is to provide the silibinin double-layer slow-release tablets with characteristics of good patient compliance, low side effect, rapid effect, and lasting maintenance of stable effective blood drug level. The present invention further discloses a preparation method for the silibinin double-layer slow-release tablets. The method of the present invention has characteristics of good reproducibility and high production efficiency, and is suitable for industrial mass production. In addition, the prepared double-layer slow-release tablets have good release uniformity.
WO2011152658A3 Pharmaceutical composition comprising piperazine dithioctate and glimepiride The present invention relates to a pharmaceutical composition for treating or preventing type II diabetes mellitus comprising piperazine dithioctate and glimepiride, which is a new combination drug. The pharmaceutical composition of the present invention has strong synergistic effects for treating type II diabetes mellitus by improving metabolic disorders and insulin resistance of diabetic patients as well as lowering blood glucose levels, and by increasing glucose uptake in cells, compared with single treatment of piperazine dithioctate or glimepiride, or combination treatment of thioctic acid and glimepiride.
CN101574425A Child cough granule and preparation method of same The invention discloses a child cough granule prescription used for eliminating phlegm and relieving cough for children and a preparation method of the product. The preparation method is characterized in that the child cough granule is prepared by choosing proper excipients on the basis of maintaining the base prescription of child cough syrup. The invention provides a novel preparation formulation which is taken more conveniently and safely and has same curative effect for clinical medication, and has good controllability and stability of preparation technology quality.
CN1954839B Medical composition prepared by caulis Marsdeniae Tenacissimae, ginseng and astragalus root A composite medicine for preventing and treating tumor, liver injury and infection is proportionally prepared from caulis marsdeniae tenacissimae or its extract, ginseng or its extract, and astragalus root or its extract. Its preparing process is also disclosed.
EP2275107A2 Combinations for the treatment of diseases involving cell proliferation The present invention relates to a pharmaceutical composition for the treatment of diseases which involve cell proliferation. The invention also relates to a method for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, optionally in form of its tautomers, racemates, enantiomers, diastereomers and the mixtures thereof and optionally in form of the pharmacologically acceptable acid addition salts, solvates, hydrates, polymorphs, physiologically functional derivatives or prodrugs thereof and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.
CN103070872A Medicine preparation for treating postmenopausal osteoporosis The invention provides a medicine preparation for treating postmenopausal osteoporosis and belongs to the technical field of medicines. The medicine preparation contains alfacalcidol, tibolone and necessary pharmaceutical excipients. The medicine preparation for treating postmenopausal osteoporosis, provided by the invention, has the advantages of good disintegration, good absorbing degree, high bioavailability, quick curing effect and convenience for taking. Pharmacological actions of the alfacalcidol and the tibolone can be taken to a maximum extent, the defect of single preparation in efficacy is compensated, and the medicine preparation is an excellent medicine preparation for treating the postmenopausal osteoporosis.
WO2011129379A1 Novel anti-hsp90 monoclonal antibody Disclosed are: an anti-HSP90 antibody; and use of the antibody. More specifically disclosed are: an anti-HSP90 antibody capable of recognizing cell surface HSP90; a vaccine containing the antibody; a medicinal agent comprising the antibody; an adjuvant comprising the antibody; a method for detecting a cell that is expressing HSP90 on the surface thereof, which utilizes the antibody; and others.
CN102698244A Drug composition used for preventing piglets from diarrhea and promoting piglets to grow The utility model discloses a drug composition used for preventing piglets from diarrhea and promoting the piglets to grow. The drug composition comprises the following components in percentage by weight: 4 to 6% of quinocetone, 8 to 12% of albumin tannate, 2 to 5% of gamma-aminobutyric acid, 1 to 3% of sweetener and 14 to 82% of nano-montmorillonite. The drug composition provided by the invention is different from antibiotic agents, prevents the piglets from diarrhea by the means of protecting intestine mucosa, relieving dehydrated acidism and acid-base imbalance, and alleviating abdominal pain caused by diarrhea, can be used for preventing and treating diarrhea of the piglets caused by various reasons such as bacteria, virus, mould, nutrition and stress in a non-specificity manner, can not generate bacterial drug resistance, can not threaten human health, has a remarkable therapeutic effect, is suitable for preventing diarrhea of the piglets caused by various reasons, and has a wideapplication range; and moreover, the drug composition provided by the invention can improve the feed intake of the piglets and promote the piglets to grow.
EP1214324B1 MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPases) The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula (1) are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP, wherein n, m, X, R1, R2, R3, R4, R5, R6, and R7 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
CN103054872A Meloxicam pharmaceutical composition and preparation method thereof The invention discloses a meloxicam pharmaceutical composition and a preparation method thereof. The meloxicam pharmaceutical composition comprises the following ingredients in percentage by weight: 2-10% of effective component, namely, meloxicam, 70-80% of filling agent, 7-11% of disintegrating agent, 2-5% of adhesive, 0.2-0.8% of solubilizer, 0.2-5% of lubricant and a moderate amount of solvent. Due to the reasonable auxiliary material selection and ratio distribution of the meloxicam pharmaceutical composition disclosed by the invention, the in-vitro dissolution of a meloxicam tablet prepared from the meloxicam pharmaceutical composition is significantly improved; and meanwhile, by using a preparation method of wet granulation, the tablet prepared from the meloxicam pharmaceutical composition disclosed by the invention is attractive in appearance, good in granule flowability, strong in abrasion resistance and good in compression shaping ability; due to the optimization of the preparation method and the process, the stability of the medicine in the production process is ensured, and the product quality is improved.
WO2011056957A3 Enzyme inhibiting compounds The present invention is directed to compounds that are specifically structured to provide enzyme inhibition. In specific embodiments, the enzyme inhibiting compounds exhibit antifolate activity. Particularly, the inventive compounds are formed of an antifolate residue that is active in inhibiting one or more of TS, DHFR, GARFT, and AICAR Tfase. The enzyme inhibiting compounds are useful in a variety of methods of treatment, including treating abnormal cell proliferation and treating inflammation.
EP2616072A1 Azabenzothiazole compounds, compositions and methods of use Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of 5 manufacturing a compound of Formula I.
CN1903284A Micro-pills of Niuhuang Shangqing Wan Contg. calculus Bovis, and its prepn. method A cow-bezoar microbolus for clearing away heat of the upper part of the body, an improvement on cow-bezoar bolus for higher curative effect, features that is contains the promoter chosen from microcrystalline cellulose, superfine silica gel powder, polyvidone, cross-linking polyvidone and compressible starch beside the components said cow-bezoar bolus has. Its preparing process is also disclosed.
CN101084904A Cefixime sustained-release double-layer tablet The invention relates to cefixime sustained release double layer tablet, which comprises tocefixime quick-release layer and cefixime slow release layer. Cefixime disperses in quick-release layer and slow release layer according to proper ratio, wherein cefixime or its medicinal salt or hydrate in sustained release layer has a release time over 12h.The inventive sustained release double layer tablet provides higher initial blood concentration and more ideal concentration versus curve, improves bactericidal action and reduces drug tolerance.
EP1912978A2 Ppar / agonists and processes of preparing This invention provides a method for preparing compounds having the structure [Formula (I)] wherein L is [Formula (A)] or [Formula (B)] in which R1 is hydrogen or optionally substituted alkyl, n is zero or 1 and m is 1; wherein R is H, halogen, optionally substituted C1-6alkyl or C1-6alkoxy; wherein Z is a bond, O or S; wherein p is an integer from 1 to 5; wherein Q is a bond provided that Z is not a bond when p is 1; or Q is O, S or -C(O)NR6- in which R6 is hydrogen, optionally substituted alkyl or cycloalkyl; or Q is -NR6-, -NR5C(O)NH- or -NR5C(O)O- in which R5 is hydrogen, alkyl or aralkyl provided that p is not 1; wherein W is cycloalkyl, aryl or heterocyclyl; or W and R6 form a 9-to 10-membered bicyclic ring, which may be optionally substituted or may contain oxygen, nitrogen or sulfur.
CN101284853A Carbohydrate derivates, transient metal complex compounds, method for preparing same and use on treating cancer The invention relates to carbohydrate derivatives and transition metal complex and a method for making the same as well as the use in curing cancer, in particular to Schiff base derived from carbohydrate, amine obtained after the Schiff base is reduced and coordinated transition metal complex, use and a method for making the same. The method comprises the following steps that: (1) at the temperature of between 20 and 200 DEG C, Alpha-D-mannopyranoside-3-hexanediamine is reacted with ortho-hydroxyl aromatic aldehyde to make Schiff base; (2) at the temperature of between 20 and 200 DEG C, the Schiff base is reduced to obtain diamine by sodium borohydride; (3) at the temperature of between 20 and 200 DEG C, the diazo compound made by the steps (1) and (2) is reacted with transition metal salt to make transition metal complex. In addition, the invention also relates to an application of the coordinated transition metal complex of the carbohydrate in asymmetric catalysis and medicine as well as in medicine combination used in human cancer therapy.
CN1726907A Method of preparing medication for preventing and curing hyperlipoidemia by using flavones picking up from marc of blueberry A process for preparing the medicine from the flavone extracting from the dregs of vaccinin fruit (FFV) to increase the level of HDL-C, decrease the level of TC and prevent and treat hyperlipemia includes such steps as mixing said FFV, microcrystalline cellulose, hydroxypropyl cellulose sodium, carboxymethyl starch sodium and magnesium stearate, stirring, and tabletting or filling it in capsules.
US20100136001 Methods and compositions for the treatment and diagnosis of vascular inflammatory disorders or endothelial cell disorders Disclosed herein are methods for treating a vascular inflammatory disorder or endothelial cell disorder using inhibitor compounds that inhibit the expression or biological activity of Tie-1, Tie-1 endodomain, thrombin, VEGFR2, VEGFR2 endodomain, EphA2, and any of the cytokines or kinases that are upregulated by activation of Tie-1 or thrombin, as provided herein. Also disclosed are the use of combinations of inhibitor compounds or the use of an eNOS activator compound in combination with any one or more of the inhibitor compounds. Also disclosed are methods for inhibiting the pro-coagulant activity of thrombin using a Tie-1 or Tie-1 endodomain inhibitor compound or an EphA2 inhibitor compound. Methods for diagnosing and monitoring vascular inflammatory disorders or endothelial cell disorders that include the measurement of any of the polypeptides or nucleic acid molecules of the invention are also disclosed.
EP1496868A1 Controlled release pharmaceutical compositions of carbidopa and levodopa The present invention relates to controlled release pharmaceutical compositions of carbidopa and levodopa that include a combination of different molecular weight cellulose ethers and in particular, hydroxypropyl cellulose ether.
CN103142629A Application of neohesperidin as antidepressant drug The invention discloses application of neohesperidin as an antidepressant drug. Dosage forms of the drug comprise pharmaceutically acceptable dosage forms, such as tablets, capsules, solutions, suspensions, injections and infusion solutions. The drug consists of neohesperidin and pharmaceutically acceptable aglycone and secondary glycoside of neohesperidin which are produced through hydrolysis or enzymolysis and comprises various drug dosage forms which are prepared in a manner that the drug is combined with pharmaceutical carriers. The drug has little toxicity and is free from the disadvantages of conventional antidepressant drugs, such as excited anxiety, constipation, anuresis, dizziness, sleepiness and tremor.
US8314115 Method of treating movement disorders using barbituric acid derivatives A method of treating movement disorders comprises administering to a human or animal subject in need of treatment a therapeutically effective amount of at least one compound according to the following formula: wherein R3 and R4 are each independently selected from the group consisting of lower alkyl, phenyl and lower alkyl substituted phenyl, and R1 and R2 are each independently either a hydrogen atom or a radical of the formula wherein R5 and R6 are each independently selected from the group consisting of H, lower alkyl, phenyl and lower alkyl substituted phenyl, its pharmaceutically acceptable salts, prodrugs or metabolites thereof.
US20110263649 Crystalline form of lenalidomide and a process for its preparation The present invention relates to a novel crystalline form of lenalidomide having formula (I) and chemically known as 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to a process for the preparation of said novel form and its use in pharmaceutical preparations for the treatment of autoimmune disease, inflammation, inflammatory disease and diseases such as cancer, in particular the management of multiple myeloma.
CN1875937A A sustained release injection carrying clorfarabine and cytotoxic drug Disclosed is an anticancer slow release injection carrying both clofarabine and cytotoxic drugs, which comprises slow release micro-balloons and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents include clofarabine and cytotoxic drugs selected from adriamycin, pidorubicin, Melphalan, 4-hydroperoxycyclophosphamide, actinomycin D, Vinorelbine, Tamoxifen, Tallimustine, Atrimustine, Semustine and ranimustine, the slow release auxiliary materials are selected from polylactic acid and copolymer, monomethyl polyethylene glycol, polyethylene glycol and polylactic acid copolymer, EVAc, aliphatic acid and sebacylic acid copolymer, The viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose.
CN1840058A Navel administered medicine for treating acute leukemia The invention provides a navel administered medicine for treating acute leukemia, which is prepared by mixing the following raw material herbs (by weight percent): Biden bipinnata extract 18-23%, areca seed 15-20%, airpotato yam 18-23%, borneol 8-12%, earthworm 8-12% and natural indigo 15-20%.
CN102836149A Composition used for inhibiting tumor cell proliferation, and application thereof The invention discloses a composition used for inhibiting tumor cell proliferation, and an application thereof. The composition is composed of quercetin and resveratrol. The molar ratio of quercetin to resveratrol is related to the ratio of 50% effective concentrations (EC50) of quercetin and resveratrol independently. The composition provided by the invention can be used for preparing any product of: (1) eukaryote tumor cell proliferation inhibitors; (2) medicines used for preventing and/or treating tumors; (3) health-care products; (4) foodstuffs; and (5) nutrient supplements. As a result of tests, a tumor cell proliferation inhibiting effect of the composition is substantially higher than that of single quercetin or single resveratrol. A combination index CI is lower than 1, such that the two components have a synergetic effect. When a same effect is reached, the dosage concentration of a single component in the composition is reduced, thus the possible potential toxicity to host normal cells is reduced.
WO2009156458A1 Novel phenolic and catecholic amines and prodrugs thereof The present invention relates to novel phenolic and catecholic amines of Formula 1, to processes for their preparation, pharmaceutical compositions containing them, to their use in therapy and to their use in radiolabeled form as PET- or SPECT Iigands.
WO2009153319A1 Anti-tumour compositions and methods A method for the prophylaxis and/or treatment of a tumour in a subject is provided. The method comprises the steps of administering a therapeutically effective amount of a composition comprising an anti- tumour agent and a therapeutically effective amount of a composition comprising 5-[2-pyrazinyl]-4-methyl-1,2-3-thione, or an analogue, derivative, metabolite, prodrug, solvate or pharmaceutically acceptable salt thereof to the subject. Examples of anti-tumour agents for use in the method of the invention are platinum-based agents, such as cisplatin, and monoclonal antibodies, such Cetuximab. Also provided are compositions comprising an anti-tumour agent and 5-[2-pyrazinyl]-4-methyl-1,2-3-thione, or an analogue, derivative, metabolite, prodrug, solvate or pharmaceutically acceptable salt thereof.
US20120202888 Biomarkers of prostate cancer and predicting mortality Measurement of circulating C-peptide levels is useful for the prognostic evaluation of subjects, in particular for the prediction of adverse clinical outcomes, e.g., mortality, and the detection of fatal prostate cancer.
EP0960127B1 Isolated dimeric fibroblast activation protein alpha, and uses thereof The invention involves dimeric forms of the protein known as fibroblast activation protein alfpha, or 'FAPα' and its uses.
EP1526859A1 Process for preparing a sterile high molecular weight hyaluronic acid formulation A process for preparing a sterile ready-to-use aqueous pharmaceutical formulation comprises a high molecular weight hyaluronic acid salt (HA) at a specified concentration, comprising the steps of: providing an aqueous formulation comprising high molecular weight HAat a concentration of less than the specified final concentration; passing said aqueous formulation through a filter having a pore sizeless than 0.45 pm; concentrating said aqueous formulation by applying a vacuum and boiling off water until said specified concentration is reached.
CN102488673A Probucol nanometer dispersion and preparation method thereof The invention provides a probucol nanometer dispersion and a preparation method thereof. The particle diameter of probucol is below 3 microns, the average diameter is below 800nm, and the stability is good. The preparation method comprises the following steps: mixing a probucol raw medicine of different types and concentrations of stabilizer aqueous solutions, and using a planetary ball mill to grind and disperse through the liquid-adding ball milling method. The technologies such as freeze drying and spray drying are adopted to dry the nanometer mixed suspension, and solid preparations such as tablets, capsules and dry suspension are prepared through further processing.
US20090221641 Diaza-spiro--nonane derivatives as neurokinin (nk1) antagonists This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonist ic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nocicept ion, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
US7300950 Pyrazole derivatives, their preparation and their use in pharmaceuticals The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate “cGMP” and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.
WO2008120778A1 Composition for promoting ketone compound formation It is intended to provide a composition for promoting the formation of a ketone compound which contains a water-soluble β-hydroxy short to medium chain fatty acid polymer. This composition for promoting the formation of a ketone compound is appropriately usable in preventing and treating various diseases which can be prevented or treated by promoting the formation of a ketone compound.
CN101269076A Medicine use of beta-methoxy acrylic ester compounds as novel STAT3 restrainer The invention relates to the application of compounds possessing STAT3 inhibitor activity shown in general formula I, isomers and a drug compound containing the compounds and isomers in the prevention or treatment of malignant tumors, AIDS and inflammations and the termination of unexpected pregnancies or the application of tool drugs used for studying the growth, proliferation, differentiation and apoptosis of tumors as well as STAT3-related signaling pathways.
US20100273870 Compositions and methods for treating demodex infestations Compositions containing about 0.6% to about 20% of tea tree oil are described. Some compositions are in the form of solutions, suspensions, spray, lotions, gels, pastes, medicated sticks, balms, cleansers (including shampoos and soaps), creams, or ointments. Also described are compositions and methods for use in treating ocular Demodex infestations and related conditions using such compositions.
CN103040772A Repaglinide dispersible tablet and preparation method thereof The invention relates to a repaglinide dispersible tablet and a preparation method thereof. The dispersible tablet comprises the following components in percentage by weight: 3 to 30 percent of repaglinide or salt thereof, and 97 to 70 percent of pharmaceutical excipient. According to the preparation, active components can be quickly dissolved and play effects, so that the bioavailability can be improved; and the medicament application safety can be improved due to high stability.
CN101914074B Thiazole-substituted mercaptoacetamide derivative, preparation method and application thereof The invention belongs to the technical field of medicines, and in particular discloses thiazole-substituted mercaptoacetamide compounds shown as the formula I, N-oxides, stereoisomers, a stereoisomer mixture, pharmaceutically acceptable salts, hydrate thereof, and a solvation matter, polycrystals and eutectics thereof, precursor and derivatives with same biological function, a preparation method thereof and application of a composition containing one or more compounds to treating and preventing human immunodeficiency virus (HIV) and influenza virus infection.
US20080146524 Such as 3-[Hydroxy-(3-phenyl-butyl)-phosphinoyl]-propionyl)-2-amino-(3-methyl-butyrylamino)hexcanoic acid; intermediates; potent and selective endopeptidases inhibitors Embodiments of this invention relate to compounds that are selective inhibitors of neurotensin degrading enzymes, to pharmaceutical compositions containing these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions containing these compounds. The invention also relates to the use of such compounds and compositions for regulating blood pressure or gastric emptying, or treating Parkinson's disease, anxiety, depression, or psychosis. The compounds have the formula (1) wherein the symbols have the meanings given in the specification.
US20070275995 Thiobenzimidazole derivatives The present invention is a thiobenzimidazole derivative represented by the following formula (1) or a medically acceptable salt thereof wherein said thiobenzimidazole derivative and a medically acceptable salt thereof have a potent activity of inhibiting human chymase. Thus, they are potential preventive and/or therapeutic agents clinically applicable to various diseases in which human chymase is involved.
EP1492756A1 Novel thyroid receptor ligands This invention relates to novel compounds according to the general formula : which are thyroid receptor ligands, preferably antagonists, partial antagonists or partial agonists and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyro-toxicosis, subclinical hyperthyrodism and liver diseases.
US20080070989 Method of Evaluating Evenness of Suplatast Tosilate Crystal, Even Crystal, and Process for Producing the Same Provided are a method for evaluating evenness of suplatast tosilate crystals; stable suplatast tosilate crystals exhibiting evenness in optical purity; and a method for producing the suplatast tosilate crystals. The method for evaluating evenness of suplatast tosilate crystals includes: (a) a step of adding a solvent to suplatast tosilate crystals to thereby dissolve 3% or less of the crystals in the solvent, and subjecting a portion of the supernatant of the resultant suspension to optical purity measurement, and (b) a step of adding a solvent to the remaining suspension to thereby dissolve the entirety of the suspension in the solvent, and subjecting a portion of the resultant solution to optical purity measurement, wherein the optical purity as measured in the step (a) is compared with the optical purity as measured in the step (b). The suplatast tosilate crystals exhibits excellent evenness and thermal stability. The method for producing the suplatast tosilate crystals is also provided.
WO2014000586A1 Phenanthroindolizidine alkaloid derivates and salt thereof as well as preparation, plant-virus resisting activity, and anti-cancer activity of phenanthroindolizidine alkaloid derivates and salt thereof Provided are phenanthroindolizidine alkaloid derivates and salt thereof as well as preparation, a plant-virus resisting activity, and an anti-cancer activity of phenanthroindolizidine alkaloid derivates and salt thereof. The derivates and the salt thereof have a good plant-virus resisting activity, which is capable of well restraining a tobacco mosaic virus (TMV), and meanwhile, have a good anti-cancer activity, which is capable of well restraining the human lung adenocarcinoma A-549 and the human leukemia HL-60.
CN102343100A Method for quickly preparing rutin inclusion compound The invention discloses a method for quickly preparing a rutin inclusion compound. In the method, the rutin inclusion compound is prepared by adopting a ball milling technology, so that the formation time of the inclusion compound is reduced to 2 hours, the preparation method is shortened greatly and the working efficiency is increased. The method mainly comprises the following steps of: preparing beta-cyclodextrin or a derivative thereof into a saturated solution at the room temperature, wherein the solution can be heated to clear state; weighing 10-50 milligrams of rutin for adding into every milliliter of saturated solution of beta-cyclodextrin or the derivative thereof, and heating and dissolving with an appropriate amount of methanol; quickly pouring a rutin solution into the solution of beta-cyclodextrin or the derivative thereof, mixing uniformly, pouring into a ball mill, performing ball milling at the rotating speed 30-200 r/min for 0.5-2 hours, and refrigerating; and performing suction filtration and drying to obtain a faint yellow powdery rutin inclusion compound. The solubility of the prepared inclusion compound is over 0.55 mg/ml, which is increased by more than one time in comparison to that of rutin, the bioavailability of a rutin oral liquid is improved, and the treatment effect is enhanced.
CN102335366A Oral liquor for treating psoriasis and preparation method thereof The invention discloses an oral liquor for treating psoriasis and a preparation method thereof. The oral liquor is prepared from divaricate saposhnikovia root, scutellaria baicalensis, anemarrhena asphodeloides, tree peony bark, tribulus terrestris, cogongrass rhizome, cortex dictamni, kochia scoparia, indigowoad root, south dodder seed, Polygonum multiflorum, glossy privet fruit, Salvia miltiorrhiza, red paeony root, astragalus mongholicus, glabrous greenbrier rhizome, dried rehmannia root, licorice root, broken and packed gypsum, Sinkiang arnebia root, Chinese trumpet creeper, crude flos sophorae, folium isatidis and safflower water by decoction and concentration. The oral liquor for treating psoriasis has obvious effects of clearing heat and cooling blood, detoxifying and removing ecchymosis, nourishing Yin and moistening dryness, removing dampness and expelling wind, promoting blood circulation and removing blood stasis, killing parasites and relieving itching as well as tonifyingliver and kidney, and psoriasis is not easy to relapse.
WO2005000405A3 P38 kinase inhibitor compositions and methods of use Methods of treating an individual who has been identified as having been infected with HIV are disclosed. Methods of treating an individual who is suspected of having been exposed to HIV are disclosed. Some methods disclosed comprise the step of administering to the individual an amount of a p38 inhibitor effective to inhibit FasL expression. Some methods disclosed comprise the step of administering to the individual an amount of a p38 inhibitor effective to inhibit HIV replication. Some methods disclosed comprise the step of administering to the individual an amount of a p38 inhibitor effective to inhibit HIV replication without inhibiting T cell activation. Some methods disclosed comprise administering to the individual one or more other anti-HIV compounds in combination with a p38 inhibitor. Methods of identifying compounds that inhibit Nef mediated upregulation of FasL expression are disclosed. Methods of identifying compounds that inhibit the p38 pathway are disclosed.
US7538118 6-aminomorphinane derivatives, method for production and use thereof This invention relates to compounds of the formula (I).
CN103360327A Benzophenazine derivative, as well as preparation method and application thereof The invention belongs to the fields of medicaments and chemical industry and discloses a benzophenazine derivative, as well as a preparation method thereof and an application thereof as an anti-cancer medicament. The benzophenazine derivative is as shown in the structural formula (I), wherein R1 and R2 are H, halogen, -OCH3 or -NO2; R1 and R2=-O-CH2-O-; n=1 or 2; and R represents various aliphatic amines and comprises chain-like and cyclic aliphatic amines. The invention simultaneously discloses the preparation method of the benzophenazine derivative and the application thereof as the anti-cancer medicament. The benzophenazine derivative has a very strong inhibitory effect against topoisomerase I and topoisomerase II, has a significant inhibitory effect against various cancer cell strains, and has a broad application space in preparation of anti-cancer medicaments.
US20100298242 Masking the taste of compositons containing salt The invention relates to the use of sweeteners for masking the salty taste of compositions as well as compositions containing salt and defined sweeteners, the amount of sweeteners being suitable for masking the salty taste of the composition.
WO2006101105A1 Agent for treatment of psoriasis Disclosed is an agent for treatment and/or prevention of psoriasis which contains a thiadiazoline derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof. [In the formula, n represents an integer of 1-3; R1 represents a hydrogen atom and R2 represents a lower alkyl, or alternatively R1 and R2 combine together to form an alkylene; R3 represents a lower alkyl; R4 represents NHSO2R6 (wherein R6 represents a hydroxy or the like) or the like; and R5 represents an aryl or the like.]
CA2614518A1 Dicycloalkyl urea glucokinase activators Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes. (I)
US20100028338 Gimatecan (7-t-butoxyiminomethylcamptothecin) and chemotherapeutic agents A combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis is disclosed. The patient is treated with a camptothecin derivative and one or more chemotherapeutic agents selected from a microtubule active agent; an alkylating agent; an anti-neoplastic anti-metabolite; a platin compound; a topoisomerase II inhibitor; a VEGF inhibitor; a tyrosine kinase inhibitor; an EGFR kinase inhibitor; an mTOR kinase inhibitor; an insulin-like growth factor I inhibitor; a Raf kinase inhibitor; a monoclonal antibody; a proteasome inhibitor; a HDAC inhibitor; and ionizing radiation.
EP2597972A1 Use of a mixture of probiotic bacteria in a mixture with short - chain fatty acids Use of a mixture live cultures probiotic bacteria in a mixture with short chained fatty acids (SCFA), in a slow release form for the active ingredients, of various release structures and mechanisms, in particular in the form of a triglyceride matrix; in the diet of monogastric animals, in particular a human diet, for modulating intestinal bacterial flora as well as improving the acid-base and water-electrolyte balance of the gastrointestinal tract; in the manufacturing of a preparation for maintaining bacterial and acid-base homeostasis of the distal portion of the gastrointestinal tract of monogastric animals, including the human small intestine and colon.
WO2008031509A1 ISOSERINE DERIVATIVES FOR USE AS COAGULATION FACTOR IXa INHIBITORS The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood coagulation factor IXa, to methods for producing the same and to the use thereof as drugs.
US20110160223 NMDA Receptor Antagonists for the Treatment of Neuropsychiatric Disorders Provided are pharmaceutical compositions and methods of treatment or prophylaxis of certain neuropsychiatric conditions, in particular mood disorders. The compounds are of the general Formula I-V as described herein.
CN103655548A New use of proanthocyanidin B2 The invention relates to the technical fields of medicines, healthcare products and the like, and discloses a new use of vegetable active component related proanthocyanidin B2 in the preparation of products, especially medicines and healthcare products, used for preventing, diagnosing, detecting, protecting, treating and researches vascular dementia diseases and direct related diseases thereof. Experiments confirm that the proanthocyanidin B2 can improve the learning and memory ability of mice with vascular dementia caused by cerebral ischemia reperfusion lesion and rats with vascular dementia caused by focal cerebral ischemia-reperfusion. The above compound has the advantages of strong effect, obvious effect, abundant sources, stable properties, use safety, especially wide application range, and furthest effect performance. The proanthocyanidin B2 can generate obvious social and economic benefits in a short time with after popularization with the continuous increase of the incidence of dementia.
US20120329819 New crystalline form of pemetrexed disodium The present invention relates to a new polymorphic or crystalline form of Pemetrexed Disodium, processes for its preparation and its use, in particular for the preparation of medicaments.
CN101422443A Fenofibrate osmotic pump controlled release preparation and preparation method thereof The invention belongs to the field of medicament preparation and discloses a fenofibrate osmotic pump type controlled release preparation and a preparation method thereof. The preparation is formed by an osmotic pump tablet core and a controlled release coat coated outside the tablet core. The weight of the osmotic pump controlled release tablet core is as follows: 250mg/tablet of fenofibrate, 25mg to 100mg/tablet of osmotic active matter, 200mg of 300mg/tablet of accessory which can lead the medicament in a medicine containing layer to be easily released, 75 to 150mg/tablet of accessory which leads the medicament to be easily released in a promoting layer and proper amount of other accessories. The weight of the osmotic pump coat is as follows: 15g to 30g/100 tablets of semi-transparent membrane coat macromolecule material and 2 to 10g/100 tablets of pore-foaming agent. The invention can effectively adjust the release speed of the medicament by adjusting the tablet core and the prescription of the coat and obtain more stable and durable effective blood medicine concentration, thereby reducing the side effect and the taking times of the medicament, ensuring that the suction of themedicament is not affected by whether the patient eats or not and the environment in a body, and improving the compliance of a sufferer. The invention can be broadly applied to curing hyperlipemia.
WO2011144787A1 Use of phenolic compounds for the treatment of helicobacter pylori-induced diseases The invention relates to a series of phenolic compounds which can be extracted from grapes or wine and which have a bactericidal capacity against Helicobacter pylori, as a result of which said compounds can be used to produce a drug for the treatment and/or prevention of diseases caused by this bacterium or as additives in functional foods or food products.
US20100278921 Solid oral formulation of abt-263 An orally deliverable pharmaceutical composition comprises (a) a pharmaceutically acceptable acid addition salt of ABT-263 in solid particulate form, and (b) a plurality of pharmaceutically acceptable excipients including at least a solid diluent and a solid disintegrant; wherein the salt is formed from more than one equivalent of acid per equivalent of ABT-263. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
WO2012167226A3 Method, composition, and articles for improving joint lubrication Articles for increasing lubrication of a joint are described herein. The articles include resorbable, biocompatible particles having a glass transition temperature within a joint of less than about 37°C and capable of increasing fluid movement within the joint compared to synovial fluid, viscosupplemental fluid, or combinations thereof. A composition for increasing lubrication of a joint is also disclosed. The composition includes the resorbable, biocompatible particles and a carrier fluid. Methods of lubricating a joint and treating disease affecting the joint such as osteoarthritis are also described herein. The methods include introducing the resorbable, biocompatible particles into a joint.
WO2013067749A1 Use of (-)-epigallocatechin gallate Disclosed is the use of (-)-epigallocatechin gallate for preparing drugs for treating or preventing tumours. (-)-Epigallocatechin gallate is abbreviated as EGCG. The drug is extracted from tea leaves. The drug and inhibitor thereof can inhibit the abnormal activation of the NOTCH signal, and are suitable for the treatment of tumours related to abnormality of the NOTCH signal.
CN101386607A Taxane derivatives, preparation method and applications thereof The invention relates to new taxane derivatives, which are prepared from taxane compounds (taxol, docetaxel or 9-dihydro-taxol), organic acids with completely acetylated alcohol hydroxy, and 4-dimethylamino-pyridine and dicyclohexyl carbodiimide used as catalysts together through esterification reaction. The effects of pharmacological tests show that the derivatives have stronger cytotoxic biological activities to various human cancer cell lines and have broad-spectrum anti-tumor effects, and the tumor inhibiting effect of the derivative in mice is superior to that of the taxol and the docetaxel obviously. Toxicity tests also show that the toxicity of the derivatives is obviously reduced compared with the taxol and the docetaxel, which improves the safety in clinical application. Therefore, the taxane derivatives are effective anti-tumor agents, which can be applied to the preparation of anti-tumor drugs.
EP2396039A2 Ultrasmall superparamagnetic iron oxide nanoparticles and uses thereof The present invention provides biomimetic contrast agents, dual functional contrast agents effective for therapeutic gene delivery and magnetic nanoparticles which comprise functionalized iron oxide nanoparticle cores, one of an inert gold layer, a layer of inert metal seeds or a silica layer and, optionally, one or both of an outer gold-silver nanoshell or a targeting ligand attached to the inert gold layer or the gold-silver nanoshell. Also provided are methods of in vivo magnetic resonance imaging, of treating primary or metastatic cancers or of ablating atherosclerotic plaque using the contrast agents and magnetic particles. In addition, kits comprising the biomimetic contrast agents, dual contrast agents and magnetic nanoparticles.
CA2120001C Flavopereirine-based pharmaceutical composition and use thereof for treating hiv A composition comprising flavopereirine, or a salt or other pharmacologically acceptable derivative thereof, as the only active principle. The composition is a solid containing around 250-500 mg of the active principle, which may be administered orally in daily doses of around 1-3g. Said composition may be used for treating humans affected by HIV-1 and people with AIDS.
WO2014074700A1 Antagonists of gpr119 receptor and the treatment of disorders related thereto The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are antagonists of GPR119 useful in the treatment of, for example, a disorder selected from: obesity and diseases/conditions related to obesity such as congestive heart failure, polycystic ovarian syndrome, infertility, gastroesophageal reflux disease, cholelithiasis (gall stones), hernia, erectile dysfunction, urinary incontinence, chronic renal failure, lymphedema, osteoarthritis, hyperuricemia, lower back pain, stroke, headache, asthma, and immobility. In addition, the present antagonists of GPR119 are useful for treating non-alcoholic fatty liver disease, food-dependent Cushing's syndrome, and cancer (e.g., cancers of the esophagus, uterine lining, ovary, kidney, pancreas, and breast; leukemia, multiple myeloma, non-Hodgkin's lymphoma, and colorectal cancer).
CN1928089A Total genome of HIV virus The present invention relates to the whole genome of one HIV strain, which has the whole nucleotide sequence as shown in SEQ ID No. 5 and partial nucleotide sequence capable of being applied in HIV vaccine design and as the important vaccine developing material. The sequence the present invention provides possesses 91-96 wt% homology to five published sequences, including U71182, DQ007902, DQ007903, DQ007901 and AY180905. The present invention features the different parts between the sequence and other B' subtype virus gene sequences, and the differences result in functional change in nucleic acid and amino acid level and direct and indirect influence on the subsequent medicine and vaccine design. The vaccine and treating medicine developed based on the sequence may result in positive effect in preventing and controlling AIDS.
CA2566041A1 T-type calcium channel splice variant compositions and methods Cell proliferative conditions are associated with expression of a previously unknown Cav3.1 T-type calcium channel splice variant, Cav3.1ac. Also, it has been determined that the Cav3.1ac T-type splice variant interacts with annexin III (ANX III). This interaction is useful in identifying substances to treat cell proliferation. Also, diagnostics and prognostics of cell proliferative disorders and methods for treating such disorders are disclosed.
US20120214843 Combination Treatment of Hydroxpyridonate Actinide/Lanthanide Decorporation Agents The invention provides for a method for treating a subject in need of such treatment comprising administering a therapeutically effective amount of one or more pharmaceutical compositions comprising a 1,2-HOPO chelating agent and a 3,2-HOPO chelating agent to a subject in need of such treatment. The use of both 1,2-HOPO and a 3,2-HOPO chelating agents in combination is more effective than using only one chelating agent alone. The invention is especially useful when practiced on a subject that has been exposed to, have been in contact with, or contaminated by one or more known or unknown actinides and/or lanthanides, or a mixture thereof.
WO2012164969A1 Pharmaceutical composition for preventing and/or treating cancer, containing substituted phenanthrene compound as active ingredient [Problem] To provide a pharmaceutical composition containing a substituted phenanthrene compound, which has a superior cancer cell proliferation inhibitory effect compared with known substituted phenanthrene compounds each having a cancer cell proliferation inhibitory effect. [Solution] The present invention is accomplished on the basis of a finding that a substituted phenanthrene compound represented by formula (I) has a superior cancer cell proliferation inhibitory effect compared with known substituted phenanthrene compounds each having a cancer cell proliferation inhibitory effect and has no adverse side effect.
WO2008021956A2 Acylaminoheteroaryl hepatitis c virus protease inhibitors The present invention discloses compounds of formulae (I) and (II), or pharmaceutically acceptable salts, esters, or prodrugs thereof: Which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering to the subject a pharmaceutical composition comprising a compound of the present invention.
CN103285325A Medicine composition for treating pressure sores The invention discloses a medicine composition for treating pressure sores. The medicine composition is made from the following medicines in parts by weight: 15-25 parts of golden yellow powder, 1-9 parts of bromogeramine tincture solution, 1-9 parts of gentian violet solution and 5-15 parts of paraffin oil. A preparation method of the medicine composition comprises the steps of respectively weighing the golden yellow powder, the bromogeramine tincture solution, the gentian violet solution and the paraffin oil in a certain parts by weight, uniformly mixing the golden yellow powder, the bromogeramine tincture solution and the gentian violet solution, finally uniformly blending by taking the paraffin oil as a softener and obtaining the paste medicine composition. The medicine composition disclosed by the invention is convenient in obtaining raw materials, simple in preparation, low in cost and good in treatment effect; the medicine composition has efficacies on the pressure sores of all stages, the effect taking rate is 100% after use and the cure rate is high; and allergy symptoms have small possibility of generation, no sequel or complication happens, the use is convenient and a novel medicine composition is provided for treating pressure sore diseases.
CN101791318A Novel application of bacterial lipopolysaccharides The invention discloses novel application of bacterial lipopolysaccharides, namely application in preparation of medicaments for dissolving foreign substances (such as thrombus, stones and tophus) in human bodies. Research shows that the bacterial lipopolysaccharides can activate the cell phagocytosis of reticuloendothelial systems, improve the bactericidal effect of macrophages and neutrophils, release endogenous cytokines (complements, properdin, lysozyme, B-lysin, interferon IFN, interleukin IL, tumor necrosis factor TNF and the like) to arouse the defense of hosts against bacterial infection cause tumor necrosis and phagocytize and dissolve thrombus, stones, tophus and other foreign substances in human bodies. Therefore, the bacterial lipopolysaccharides can be taken as active components and prepared into medicaments for preventing and/or treating strokes, stones and gout. Thalli injection containing the bacterial lipopolysaccharides proves safe and effective through animal experiment, and clinical verification shows that the effective rate of treating strokes/gout/stone diseases is 100 percent; the recovery degree of the patients with strokes can reach 50 to 90 percent; and the cure rate of the patients with stones/gout can reach 75 percent.
WO2006101104A1 Agent for treatment of arthritis Disclosed is an agent for treatment and/or prevention of arthritis which contains a thiadiazoline derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof. [In the formula, n represents an integer of 1-3; R1 represents a hydrogen atom and R2 represents a lower alkyl, or alternatively R1 and R2 combine together to form an alkylene; R3 represents a lower alkyl; R4 represents NHSO2R6 (wherein R6 represents a hydroxy or the like) or the like; and R5 represents an aryl or the like.]
CN103524564A Synthesis method and application of platinum (II) complex of 6-amino oxoisoaporphine The invention discloses a new platinum (II) complex of 6-amino oxoisoaporphine, namely monochloro.dimethyl sulfoxide.6-amino oxoisoaporphine platinum (II), and a synthesis method and an application thereof. The complex is synthesized by the steps of dissolving 6-amino oxoisoaporphine and dichloro.di(dimethyl sulfoxide) platinum (II) in a polar solvent, and heating or carrying out a reflux reaction to obtain the target product; specifically the complex can be synthesized by a solution method, and can also be synthesized by a solvothermal method. Through investigation of proliferation inhibitory activity of the complex against HepG2, BEL-7404 and NCI-H460 and other human tumor cell strains, the complex is found to have significant in-vitro antitumor activity against the 3 kinds of tumor strains and have relatively good potential medicinal value, and is expected to be used in preparation of various antitumor medicines. The complex has the chemical structure represented by the following formula as described in the specification.
CA2428438C Eukaryotic cell division genes and their use in diagnosis and treatment of proliferative diseases The present invention relates to the significant functional role of several C. elegans genes and of their corresponding gene products in cell division and proliferation processes that could be identified by means of RNA-mediated interference (RNAi) and to the identification and isolation of functional orthologues of said genes including all biologically-active derivatives thereof. The invention further relates to the use of said gene products (including said orthologues) in the development or isolation of anti-proliferative agents, particularly their use in appropriate screening assays, and their use for diagnosis and treatment of proliferative diseases.
US6969707 For therapy or inhibiting the development of a pathology associated with peroxynitrite damage This invention provides a novel class of substituted macrocyclic metallic complexes. The complexes are useful as peroxynitrite decomposition catalysts. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof are also described.
CN102026635A Pharmaceutical compositions for the treatment of warts The present invention relates to pharmaceutical compositions for the treatment, and especially topical treatment, of warts and the use thereof for the treatment of warts. Specifically, the present invention relates to pharmaceutical compositions for the treatment of warts, comprising: a) 0.1 to 10 weight % dimethicone; b) 5 to 25 weight % of one or more vegetable oils; c) one or more pharmaceutically acceptable excipients and/or carriers; d) 2 to 6 weight % urea; and e) water up to 100 weight %.
US20120029013 Derivatives of aminocyclobutane or aminocyclobutene, their method of preparation and their use as medical products The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C1-C6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3′ each independently or together are a hydrogen atom or C1-C6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.
CN1839866B Medicinal composition containing breviscapine The invention provides a breviscapinum-containing pharmaceutical composition, wherein each unit dosage of the composition comprises 50-90mg of breviscapinum and pharmaceutically acceptable carrying agent and/or excipient, the preferred content of breviscapinum in each unit dosage of the composition is 55-80mg, the preferable content is 58-75mg, and 60-70mg, the optimal content is 60-65mg. The forms suitable for the composition include preparation for injection, preparation for oral administration or preparation for external use. The composition of the present invention has the advantages of high effect, low toxicity, convenient to produce and use, low cost, and so on.
US20100298368 Antagonists of pgd2 receptors Described herein are compounds and pharmaceutical compositions containing such compounds that modulate the PGD2 activated chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2). Also described herein are methods of using such CRTH2 modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2 mediated conditions or diseases.
WO2007134827A1 5-phenyl-thiaz0l-2-yl-urea derivatives and use as pi3 kinase inhibitors The present invention concerns a compound of formula Ia wherein: Ra * is hydrogen or C1-C4-alkyl; Rb* is -(C1-C4-alkylene)-Y-C1-C4-haloalkyl or -(C1-C4-alkylene)-Y-C1-C4-hydroxyalkyl; Y represents -CONH- or a five membered heteroaryl group. R2* is C1-C4-alkyl or halogen; R3* is halo, -SO2-CH3, -SO2-CF3, carboxy, -CO-NH2, -CO-di(C1-C8-alkyl)amino, or a 5- or 6- membered heterocyclic ring having one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur, that ring being optionally substituted by halo, cyano, oxo, hydroxy, carboxy, nitro, C3-C8-cycloalkyl, C1-C8-alkylcarbonyl, C1-C8-alkoxy optionally substituted by aminocarbonyl, or C1-C8-alkyl optionally substituted by hydroxy, C1- C8-alkoxy, C1- C8-alkylamino or di(C1- C8-alkyl)amino; R4* is hydrogen, halo, -SO2-CH3, nitrile, C1- C8-haloalkyl, imidazolyl, C1- C8-alkyl, -NR8*R9*, or -SO2-NR8*R9*; and R5* is hydrogen, halogen or C1- C8-alkyl; R8* and R9* are independently hydrogen, amino, C1- C8-alkylamino, di(C1- C8-alkyl)amino, or CC1- C8-alkyl optionally substituted by hydroxyl; or a pharmaceutically acceptable salt, or solvate thereof, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
US20080021029 Substituted Cyclic Urea Derivatives, Preparation Thereof And Pharmaceutical Use Thereof As Kinase Inhibitors The disclosure relates to the novel compounds of formula (I): wherein R1, R2, R2′, R3, R3′, p, A, B, Y, Y1, and Y2 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.
CN101283979B Preparation method of hyaluronic acid small fragment plaster for promoting the wound healing The invention relates to a method for preparing hyaluronan fragment ointment for promoting wound healing. The preparation method comprises the steps of: preparing oligosaccharides of hyaluronan, identifying, separating, and purifying to obtain 4-20mers of oligosaccharides of hyaluronan fragment (o-HA); mixing glycerin monostearate, ceresin and white vaseline, melting, adding liquid paraffin, and keeping at 80 DEG C to obtain oil phase; mixing 4-20mers of o-HA, ethyl p-hydroxybenzoate, OP emulsifying agent and Span-80, adding distilled water, and keeping at 70-80 DEG C to obtain water phase; adding water phase into oil phase while stirring until emulsification completes, and condensing to obtain o-HA ointment. The o-HA ointment can effectively delay the local release of o-HA at the wound site, promote local vascularization at the wound site, and promote wound healing.
CN1634104A Sustained release mini pills of breviscapine and its preparing process Disclosed is a slow release preparation with Breviscapine as the main medicinal composition and its preparing process, wherein the slow release capsule includes drug-carrying capsuled pellets, and each 1000 grains of slow release capsule comprises Breviscapine 124g, medicinal starch 116g, crystalline cellulose 160g, the slow release capsule liquid comprises ethyl cellulose (EC: RT-20) 16g, methyl hydroxypropylcellulose (HPMC: RT-50) 2g, polyethylene glycol (PEG400) 1g, diethyl phthalate 1g, and right amount of 80% ethanol solution.
US20080026073 Method and composition for lithium additive in treatment of glutamate toxicity Treatment of glutamate toxicity is accomplished using Lithium or a composition of Lithium and a botanical extract. The composition is administered using conventional techniques to increase the survival of ganglion cells exposed to glutamate toxicity resulting from ischemic events. In exemplary embodiments, the botanical extract is St. Johns Wort, Tian Qi or Dong Gui.
WO2011001441A1 A composition of extract of emblica officinalis and method of preparing the same The present disclosure relates to a composition of an extract of fruits of Emblica officinalis selected from the group consisting of liquid juice of fruits of Emblica officinalis, a powder of an alcoholic extract of fruits of Emblica officinalis, a powder of a hydro alcoholic extract of fruits of Emblica officinalis, a powder of a water extract of fruits of Emblica officinalis, a powder of a juice of fruits of Emblica officinalis, a powder of dried fruits of Emblica officinalis, a powder of a water extract of dried fruits of Emblica officinalis, a powder of a pectinase treated water extract of fruits of Emblica officinalis, and combinations thereof; a method of preparing such compositions of extract of fruits of Emblica officinalis, more particularly which has application as a nutraceutical or pharmaceutical for increasing HDL — C levels in patients with memory loss and dementia especially in patients with neurodegenerative diseases like Alzheimer's disease and for the treatment of memory loss especially in Alzheimer's disease.
WO2013100631A1 Novel imidazopyridine derivatives as a tyrosine kinase inhibitor Provided is a novel imidazopyridine derivative having irreversible tyrosine kinase inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases or hyperproliferative diseases, immunologically mediated diseases, cancers or tumors.
WO2007086651A1 Anti-cancer agent loaded hydrophobic bile acid conjugated hydrophilic chitosan oligosaccharide nanoparticles and preparation method thereof Disclosed herein are hydrophobic bile acid- conjugated hydrophilic chitosan oligosaccharide nanoparticles with anticancer agent loaded therein and a method for preparing the same. The hydrophobic bile acid- conjugated hydrophilic chitosan oligosaccharide nanoparticles form self-aggregates in aqueous phases. With a high load of anticancer agents, the hydrophobic bile acid-conjugated chitosan oligosaccharide nanoparticles with anticancer agents loaded therein exhibit excellent cytotoxicity against cancer cells. Also, the nanoparticles release the anticancer agent in a sustained manner therefrom, thereby exhibiting anticancer activity for a prolong period of time. Therefore, the nanoparticles are very useful in cancer chemotherapy.
EP2451795A1 Compositions and methods for enhancing virus efficacy Provided are viral sensitizing compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the cytotoxicity of virus to cells. Other uses, compositions and methods of using same are also provided.
US20100143346 Treatment of Macular Degeneration An agent having progesterone antagonist properties may be used to treat eye conditions associated with pathological blood vessel formation, for example age-related macular degeneration, choroidal neovascularisation, retinal neovascularisation or corneal neovascularisation. The agent may be mifepristone.
US20100076061 Repeated administration of lentiviral vectors to respiratory cells The invention provides methods for administering lentiviral vectors to the respiratory system of a patient to treat a disease.
WO2006112362A1 Process for production of polymer-type therapeutic agent for treatment of cancer [PROBLEMS] To provide a process for polymerizing a low-molecular anti-tumor agent so that the anti-tumor agent can be accumulated in tumor tissues selectively, the process enabling to increase the molecular weight and improve the tumor-selectivity of the anti-tumor agent and to give a product with high purity in simple steps. [MEANS FOR SOLVING PROBLEMS] A process for producing a polymer-type anti-tumor agent, comprising reacting an anhydrous styrene-maleic acid copolymer with a low-molecular therapeutic agent for cancer in the absence of a condensing agent under alkaline conditions, solubilizing the resulting product, adjusting the product to pH 6 to 8, and collecting a polymeric micelle complex having the active agent contained therein by a procedure for separating a polymeric component.
WO2008017691A1 Pyridine derivatives as sodium channel blockers Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein; each of R1 to R4 is independently selected from hydrogen and C1-4 alkyl, and each of rings A and B independently is optionally further substituted by up to three substituents, each of which is independently selected from the group consisting of halogen, hydroxy, C1-4 aIkoxy, C1-4 alkyl, C1-5alkanoyl, CF3, CF3O and cyano; with the proviso that ring A must contain at least one CF3group, are useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels.
US20050063971 Monoclonal or humanized antibodies that immunospecifically bind to FGF-CX or any derivative, variant, mutant, polypeptide fragment, polynucleotide or antibody The present invention provides FGF-CX, a novel isolated polypeptide, as well as a polynucleotide encoding FGF-CX and antibodies that immunospecifically bind to FGF-CX or any derivative, variant, mutant, or fragment of the FGF-CX polypeptide, polynucleotide or antibody. The invention additionally provides methods in which the FGF-CX polypeptide, polynucleotide and antibody are used in detection and treatment of a broad range of pathological states, as well as other uses.
CN102319247A Mir-26a-targeted anti-osteosarcoma small molecular compound The invention relates to a novel anti-osteosarcoma small molecular lead compound which is synthesized on the basis of a virtual medicament screening platform on which bioinformatics is combined with a computer technology and is targeted to suppress mir-26a synthesis. The small molecular compound has the advantages of high permeability, small toxic and side effects, simple structure, easiness for synthesizing and the like. The small molecular compound can be used together with a tumor necrosis factor (TNF-alpha) to enhance the tumor killing effect of the latter, so that the small molecular compound can be used for treating osteosarcoma and can become a new anti-osteosarcoma medicament.
US20100297244 Nanodispersion The present invention provides a nanodispersion comprising nanoparticles having a mean size less than 300 nm dispersed in a vehicle comprising a water miscible solvent and water, said nanoparticles comprising one or more taxane derivative, a polymer and a surfactant comprising a mixture of fatty acids or its salts and sterol or its derivatives or its salts.
WO2008101313A1 Preparation of amino acid-fatty acid amides The present invention describes compounds produced from an amino acid molecule and a fatty acid molecule. The compounds being in the form of amino-fatty acid compounds being bound by an amide linkage, or mixtures thereof made by reacting amino acids or derivatives thereof with an appropriate fatty acid previously reacted with a thionyl halide. The administration of such molecules provides supplemental amino acids with enhanced bioavailability and the additional benefits conferred by the specific fatty acid.
WO2012109673A1 Methods of treating macular edema using antiedema therapeutics The invention provides methods of treating macular edema in a patient that include determining whether the patient has been diagnosed with or has experienced symptoms of macular edema for a predetermined period of time. If the patient has been diagnosed with or has experienced symptoms of macular edema for a predetermined period of time, the method of treatment includes administering a therapeutically effective amount of an AED to the patient. If the patient has not been diagnosed with or has experienced symptoms of macular edema for a predetermined period of time, the method of treatment optionally includes treating the patient with a therapy other than an AED. The invention further provides methods of treating macular edema in a patient using methods of and devices for administering an AED.
CN101548952A Anisodamine dry powder inhalation, preparation method and application thereof The invention discloses a anisodamine dry powder inhalation, the preparation method and the application thereof, belongs to the medicinal preparation field. The dry powder inhalation is composed by the components of: 1-100wt% of anisodamine and 0-99% of excipient. The preparation method comprises: milling the anisodamine into particles with size of 1-10mum by a jet mill; pulverizing or palletizing the excipient into particles with average size of 10-200mum; mixing the anisodamine and the excipient, collecting them into a gelatin or plastic capsule, or aluminum-plastic bubble, into a dry powder suction apparatus in storage mode to obtain the anisodamine dry powder inhalation of the invention. The anisodamine dry powder inhalation in the invention can be sued to treatment stomach and intestine angina, biliary tract spasm and smooth muscle spasmolysis; has a Fast-onset and high medicament biological availability, and is more convenient for injection.
US20060183765 Methods of treating cancer using an FPT inhibitor and antineoplastic agents Disclosed is a method of treating cancer in a patient in need of such treatment comprising administering a therapeutically effective amount of an FPT inhibitor and therapeutically effective amounts of one or more antineoplastic agents. Methods of treating non small cell lung cancer, CML, AML, non-Hodgkin's lymphoma and multiple myeloma are disclosed.
EP2491919A1 Pharmaceutical solution of taxanes comprising ph regulator and preparation method thereof A pharmaceutical solution of taxanes, its preparation method, a composition comprising said solution and its pharmaceutical combination package are disclosed. Said pharmaceutical solution comprises taxanes, a pH regulator and a solvent, wherein the pH regulator is a water-soluble acid.
WO2009118493A2 Method for the continuous synthesis of an n-acylated compound, and equipment for implementing said method The invention relates to the continuous aqueous-phase synthesis of an N-acylated compound including a unit (M1) of the formula (I) in which n is 0, 1 or 2 and R1 is an aliphatic radical, wherein said synthesis comprises: the step A of reacting a compound including a unit (M2) of the formula (II), in which M is an alkaline metal atom, with a halide acid of the formula (IV): formula (III) in which X is a halogen atom, in an aqueous solution and at a pH higher than 7 in order to form a N-acylated compound including a unit (M3) of the formula (IV); the step B of hydrolysing, at a pH lower than 7, the N-acylated compound including at least one unit (M3) and obtained during the step A, in order to form the N-acylated compound including a unit (M1); characterised in that the step A is carried out by continuously contacting in time a flow at a flow rate d1 of said halide acid of the formula (IV), a flow at a flow rate d2 of said compound including at least one unit (M2) or a mixture of compounds including at least one unit (M2), and a flow at a flow rate d3 of the alkaline aqueous solution, while maintaining the molar ratio between the acid halide of the formula (IV) and the compound including at least one unit (M2) lower than 1 and higher than or equal to 0.75, and while maintaining the pH of the medium lower than or equal to 9.5 and higher than or equal to 8. The invention also relates to equipment for implementing said method.
WO2009127059A1 Complexes of isogranulatimide and granulatimide with a cyclodextrm, formulations and their use for the treatment of cancer Formulations of amorphous complexes of compounds of formula (I), such as isogranulatimide or granulatimide, with at least one cyclodextrin are disclosed. Said formulations further comprise a water- soluble compound for inducing osmosis, such as dextrose and/or sodium chloride. Also provided are methods for preparing the aforementioned formulations and methods for delivery in in vitro and in vivo applications. The formulations may be suitable for cancer indications where it is desired to enhance the cytotoxic effectiveness of anti-cancer drugs such as DNA damaging or anti-mitotic agents. In addition, these formulations may be suitable for cancer indications where it is desired to increase the effectiveness of radiotherapy. In the compounds of formula (I), W is defined as being a group of formula (i) or (ii) in which K, E and T are independently N, CR or CZ; Q is NR2, O, S or C(R)2; R1 is R, RCO- or ArCO-; X and Y are O, H, OH or H2 and R, Z, R2 and Ar are as defined in claim 1.
US20090239878 Combinations of (a) an atp-competitive inhibitor of c-abl kinase activity with (b) two or more other antineoplastic agents The invention relates to combinations of (a) an ATP-competitive inhibitor of c-abl kinase activity with (b) two or more other antineoplastic agents for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease
US20100092509 Hypo- and Hyper- Acetylated Meningococcal Capsular Saccharides Capsular saccharides derived from serogroups W135 and Y of Neisseria meningitidis have altered levels of O-acetylation at the 7 and 9 positions of their sialic acid residues, and can be used to make immunogenic compositions. Relative to unmodifed native saccharides, derivatives of the invention are preferentially selected during conjugation to carrier proteins, and conjugates of the derivatives show improved immunogenicity compared to native polysaccharides.
US20120115893 Substituted Bicyclic Carboxamide and Urea Compounds as Vanilloid Receptor Ligands Substituted bicyclic carboxamide and urea compounds corresponding to formula (I) processes for the preparation thereof, pharmaceutical compositions containing these compounds, and a method of using these compounds for the treatment and/or inhibition of pain and other conditions mediated at least in part via the vanilloid receptor 1.
CN103405481A Medicinal composition containing staphylococcus albus and preparation method thereof The invention discloses a medicinal composition containing staphylococcus albus and a preparation method thereof. The medicinal composition is characterized by comprising the following active components in parts by weight: 20-30 parts of staphylococcus albus powder, 0.03-0.05 part of ganoderma lucidum bacterium powder, 0.005-0.01 part of berberine hydrochloride. The effects of alleviating cough and asthma and diminishing inflammation, achieved by taking the medicinal composition containing the staphylococcus albus, are more remarkable than those by taking staphylococcus albus singly, and the medicinal composition has the characteristics of high bioavailability, good stability and long preservation time, and is convenient to take.
CN103463001A Application of Neonectrolide A to preparation of medicament for treating acute gout The invention provides novel application of a compound Neonectrolide A in medicine, in particular to application of the compound Neonectrolide A to preparation of a medicament for treating acute gout. An experimental research result shows that the Neonectrolide A has a protection effect on an MSU-induced HUVEC (Human Umbilical Vein Endothelial Cells) injury acute gout model and inhibits expression of ICAM-1, and thus, the compound Neonectrolide A can be used for application to preparation of the medicament for treating the acute gout.
CN102166202A Double-layer osmotic pump controlled release tablet of gliquidone and preparation method thereof The invention belongs to the technical field of medicine preparation and provides a double-layer osmotic pump controlled release tablet of gliquidone and a preparation method thereof. The osmotic pump preparation comprises a tablet core containing the gliquidone and a semi-transparent coating film coated outside the tablet core and provided with a medicine releasing pore, wherein the tablet core comprises a medicine layer containing the gliquidone and a boosting layer; the medicine layer comprises 60 mg of gliquidone, 100-300 mg of suspension, 50-200 mg of osmotic pressure active material, 30-100 mg of pH regulating agent and 0.5-2 mg of lubricating agent; the boosting layer comprises 50-150 mg of swelling agent and 5-30 mg of osmotic pressure active material; the semi-transparent coating film comprises 10-20 g of semi-transparent high polymer material dissolved in 500 ml acetone and 2-5 g of water-soluble pore forming agent dissolved in 20 ml distilled water; the weight of the coating film is 5-10% of the weight of the tablet core; and the medicine releasing pore is punched on a medicine containing layer side of a coating tablet by a laser or mechanical drill. The double-layer osmotic pump controlled release tablet of gliquidone, provided by the invention, has the characteristics of low medicine-taking frequency, lasting action and stable curative effect.
US20100199362 Wnt ligands involved in blood-brain barrier development and uses therefor Provided are methods of diagnosing and treating vascular disorders of the CNS or disorders of the blood-brain barrier comprising the use of Wnt ligands involved in the canonical Wnt signaling pathway.
EP1802610A1 Crystalline form 2 of atrasentan hydrochloride Atrasentan Hydrochloride Crystalline Form 2, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
CN102988957A Pharmaceutical compositions and methods of using secreted frizzled related protein Pharmaceutical compositions and methods of use in regulation of mammalian bone forming activities of SFRPs (secreted frizzled-related proteins) are disclosed. SFRPs are secreted receptors for Wnts that are important polypeptide growth factors that are known to regulate fundamental biological processes like tissue polarity, embryonic development and tumorigenesis. A SFRP was isolated in human osteoblast cells and identified as SFRP-1 (also known as SARP-2) and shown to be regulated by osteogenic agents in the HOB cells in a differentiation selective manner modulating the life of osteoblasts/preosteocytes.
US7915239 Treating lameness with an osseous and/or articular component which appear in a person or animal not suffering from fractures or arthritis; horses; veterinary medicine; bone disorders, osteoarthritis The invention relates to a process for treating lameness with an osseous, articular or osteoarticular component, comprising the administration, to a human or to an animal not suffering from arthritis or from fractures, of an effective amount of a bisphosphonic acid derivative of formula: in which: R1 represents a hydrogen atom, a halogen atom, a hydroxyl, an amino, a mono(C1-C4)alkylamino or a di(C1-C4) alkylamino; R2 represents a halogen atom, a linear alkyl comprising from 1 to 5 carbon atoms which is unsubstituted or substituted with a group chosen from a chlorine atom, a hydroxyl, an amino, a mono(C1-C4)alkylamino or a di(C1-C4)alkylamino; a (C3-C7) cycloalkylamino, or R2 represents a phenoxy, a phenyl, a thiol, a phenylthio, a chlorophenylthio, a pyridyl, a pyridyl-methyl, a 1-pyridyl-1-hydroxymethyl, an imidazolyl-methyl or a 4-thiomorpholinyl, of one of its pharmaceutically acceptable salts or of one of its hydrates.
CN103340846A Arachidonic acid soft capsule and preparation method The invention provides an arachidonic acid soft capsule and a preparation method. The arachidonic acid soft capsule comprises two parts, namely, contents and a shell, wherein the contents are prepared from 80 to 130 parts of arochidonic acid oil, 2 to 6 parts of beewax, and 0.05 to 0.1 part of antioxidant compound; and the shell is prepared from 5 to 10 parts of arabic gum, 25 to 40 parts of gelatin, 30 to 50 parts of glycerinum, 15 to 30 parts of water, 0.2 to 0.5 part of covering agent, 0.05 to 0.08 part of preservative, and 1.3 to 2 parts of disintegrating agent. According to the arachidonic acid soft capsule and the preparation method, a formula is reasonable, the manufacture method is simple and convenient, the arachidonic acid can be effectively prevented from oxidizing so that the shelf life can be prolonged, the prepared product is convenient to carry and take, the effect on smell covering is great, and the problems due to the oxidation resistance, stability and disintegration of the product are solved at the same time.
CN101244047B Application of octacosanol in preparing medicament for preventing and controlling altitude erythrocytosis The invention relates to an application of octacosanol in the preparation of medicine used for preventing altitude erythrocytosis, which is characterized in that: the extracted octacosanol with the purity of 98% and the disintegrant of carboxymethyl starch are mixed together, and then are taken into a capsule, wherein, in each capsule, the octacosanol is 10mg and the disintegrant is 0.3mg. The application has the advantages of effectively preventing increase of erythrocyte caused by long-term chronic anoxia, enhancing anoxic tolerance of organism and improving microcirculation.
US6919458 Preparation of terfenadine carboxylic acid metabolite and carebastine using a 1-(2-substituted isopropyl)-4-(cyclopropylcarbonyl)-benzene compound intermediate The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety and converting the regioisomer to the piperidine derivative compound with a piperidine compound.
US7968546 Pyridazinone kinase inhibitors Disclosed are compounds of Formula I wherein X is and R2, R1, A, B, D, E, R9 are as defined herein useful for treating cancers.
WO2011057145A3 Imidazo[1,2-a] pyridine compounds, synthesis thereof, and methods of using same Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to imidazopyridine compounds, synthesis thereof, and methods of using same. Disclosed herein are various imidazo[1,2-a]pyhdine compounds and methods of using the novel compounds to treat or prevent tuberculosis in a subject or to inhibit fungal growth on plant species. Other embodiments include methods of synthesizing imidazo[1,2- a]pyridine compounds, such as the disclosed imidazo[1,2-a]pyridine compounds.
CN102784168A Calcium magnesium tablet A calcium magnesium tablet is provided and is a latest product invented at present. Heartburn is one most common problem of gastrointestinal diseases, and occurs mainly associated with the function of the sphincter at the separation place of lower esophagus and stomach. Under normal circumstances, the sphincter is in a relaxed state when people swallow, so that foods smoothly reach the stomach for digestion through the esophagus. Heartburn is a burning feeling resulted from sensitive cells, and is a symptom of case often caused by natural reflux of gastric acid to the esophagus. The calcium magnesium tablet is prepared from cuttlebone, high-calcium powder, magnesium chloride, sodium bicarbonate, and vitamin U, and plays the roles of gastric acid secretion inhibition, gastric mucosa protection, and stomach acid neutralization. People who suffer from heartburn phenomena can take the calcium magnesium tablets which have a significant therapeutic effect.
EP2616054A2 Therapy for mll-rearranged leukemia Provided are methods for treating MLL-rearranged ALL by administering to a patient an HDAC inhibitor alone or in combination with a DNA demethylating agent. Also provided are methods of treating MLL-rearranged infant ALL. Methods of treating cells by these agents are also provided. Additionally, disclosed is a method for screening for compounds capable to treat MLL-rearranged ALL, in particular, MLL-rearranged infant ALL.
WO2007116981A1 Fat accumulation inhibitor Disclosed are: an agent for inhibiting the accumulation of a fat in an adipocyte, which comprises a milk-derived phospholipid as an active ingredient; a beverage/food for inhibiting the accumulation of a fat in an adipocyte, which contains a milk-derived phospholipid; an agent and a beverage/food for inhibiting the accumulation of a visceral fat, each of which comprises a phospholipid having sphingosine or a derivative thereof as an active ingredient; and an agent and a beverage/food for promoting the increase in blood adiponectin level and/or inhibiting the decrease in blood adiponectin level, each of which comprises a phospholipid having sphingosine or a derivative thereof as an active ingredient.
WO2011028594A2 Cancer starvation therapy The present invention is a glutamine analogue which enters the mitochondrion and is subsequently exposed to ionizing radiation. When exposed to ionizing radiation, the present invention damages mitochondrial (as well as other) substructures such as mtDNA, the outer membrane, the inner membrane, cristae, ribosomes, etc., and causes the effective destruction of such mitochondrion. Tumorigenic cells without mitochondria cannot produce the energy they need to subsist and replicate, effectively starving them of energy and causing their destruction.
EP1605939B1 Pharmaceutical use of 1-azabicyclo¬ 2.2.2 octanes and a method of testing compounds for the ability of activating inactive wt p53 The present invention relates to the use of 1-azabicyclo[2.2.2]octanes, capable of transferring wild type p53 from an inactive and non-functional conformation into an active conformation, for the preparation of a pharmaceutical compositions for use in treating medical compositions wherein wt p53 exists in an inactive state defined herein, especially malignant melanoma and conditions involving undesired angiogenesis. The inven-tion also relates to methods of in vivo and in vitro testing of compounds for the above-mentioned ability, wherein inactive wt p53 is monitored or detected.
CN101829080B Application of iridoid compound to preparation of ovarian cancer resistance medicament The invention provides the application of iridoid compound to the preparation of ovarian cancer resistance medicament. The iridoid compound is isovaleric acid base dihydro valerian element or isovaleric acid base dihydro valepotriate J which has the following structural formula. The experiments on the toxic and killing effect of the isovaleric acid base dihydro valerian element or the isovaleric acid base dihydro valepotriate J on the p 53 wild ovarian cancer cells A2780, the p53 mutated OVCAR-3 cells and the normal ovarian cells IOSE144 show that the isovaleric acid base dihydro valerian element or the isovaleric acid base dihydro valepotriate J has the selective toxic and killing effect on the ovarian cancer cells and can inhibit the proliferation of ovarian cancer cells and kill the ovarian cancer cells. The iridoid compound can be used as the active component to prepare the ovarian cancer resistance medicament. The invention provides the novel ovarian cancer treatment medicament for the clinical treatment of the ovarian cancer and brings the joyous news to the patients with the ovarian cancer. The iridoid compound has higher application value.
US20080096870 Oral, intranasal or intravenous administration of bromophenylalanine and a neuroleptic agent; NMDA receptor agonists; schizophrenia; anxiolytic agents, antidepressants; Alzheimer's disease; bipolar disorder The subject invention pertains to methods of treating mental illnesses or conditions characterized by a decreased function of NMDA receptors and/or excessively enhanced glutamate release and activity of non-NMDA receptors (AMPA and/or kainate). Specifically disclosed are methods utilizing BrPhe, or isomers of analogs thereof, for treating or preventing mental illness or conditions such as schizophrenia.
WO2010063862A3 5,6-DIHYDRODIBENZO[b,f][1,4,5]THIADIAZEPINE DERIVATIVES AND THE USE THEREOF IN THE TREATMENT OF NEURODEGENERATIVE DISEASES Chemical compounds derived from the 5,6-dihydrodibenzo[b,f][1,4,5]thiadiazepine heterocyclic system and the use thereof as pharmaceutical compositions for the treatment of diseases of the central nervous system that are caused by a series of processes included in that which is generally known as neurodegeneration, specifically for the treatment of Alzheimer's disease, Parkinson's disease or Huntington's disease.
US20080292717 Highly Stable Aqueous Solution, Electrode with Nanocoating for Preparing the Solution and Method for Making this Electrode A highly stable aqueous solution having a molecular cluster with dimensions which are small enough to ensure substantial chemical-physical stability thereof for a relatively long time. To prepare the solution a fluid treatment device is used, which comprises at least one chamber (7) and at least one anode (4) and one cathode (3) arranged in the chamber (7). The anode (4) and cathode (3) are at least partly made of a first metallic material. At least one of the at least one cathode (3) and anode (4) comprises a coating of nanoparticles (5) of a second metallic material.
CN102038639A Alprostadil injection preparation The invention belongs to the technical field of medicines and discloses an injection preparation prepared from alprostadil serving as a raw material. The injection preparation is characterized by comprising the following components in part by weight: 0.01 part of alprostadil, 200 parts of soybean oil, 36 parts of phospholipid, 50 parts of glycerin and 4.8 parts of oleic acid. Through a preferable test of a preparation process, the preparation process of adjusting the pH value of foremilk to be between 5.4 and 6.0 and treating the foremilk by using a nanomachine for 5 times under the pressure of 50MPa so as to prepare lipid microspheres with the average uniform particle size of between 100 and 280nm and performing flowing steam sterilization at the temperature of 121 DEG C for 15 minutes is determined. The preparation process has the advantages of high stability, small impurity quantity and the like.
CN101229177B Medicine compounds for treating osteoporosis The invention provides a medical compound for treating osteoporosis which is characterized in that the invention contains strontium ranelate and bisphosphonate. Animal experiments indicate that the invention achieves the unexpected effect for treating the osteoporosis. The osteoporosis is a bone disease of the whole body characterized by the low bone mass and the degeneration of the micro structure of the bone organization, companying with the enhancement of the bone fragility and easy happened bone broken for which no ideal treatment medicine exists in the clinic. The bisphosphonate of the invention comprises alendronate, risedronate sodium, ibandronate, pamidronate, Etidronate, disodium clodronate and zoledronic acid, etc. In the invention, the dosage of the bisphosphonate is greatly reduced, which can effectively reduce the happening of side effects and is convenient to use the medicine.
CN102846542A Ketorolac tromethamine injection The invention discloses a prescription of a ketorolac tromethamine injection and a preparation method. The injection provided by the invention can not only effectively solve the problem that the existing ketorolac tromethamine injection containing ethanol causes irritation while being injected and improve the safety of the drugs and the compliance of the drugs, but also completely avoid the white points caused by the traditional technology after sterilization treatment, and thus the ketorolac tromethamine injection is good in stability, high in safety, reliable in quality and significant in efficacy.
US20100173958 Compounds for the inhibition of dgat1 activity Compounds of formula (I), or salts thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein, for example, R1 is optionally substituted phenyl or naphthyl; Ring A is selected from (3-6C)cycloalkyl, (5-12C)bicycloalkyl and phenyl; n is 0, 1 or 2; R2 is, for example, hydrogen, fluoro, chloro or hydroxy; Ring B is selected from (3-6C)cycloalkyl, (5-12C)bicycloalkyl and phenyl; L1 is a direct bond or a defined linker group and R3 is, for example, hydroxy, carboxy or (1-6C)alkoxycarbonyl; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
US7402598 Arylethanolamine β2-adrenoreceptor agonist compounds The present invention relates to compounds of formula (I) as defined herein and salts or solvates thereof. Processes for preparing these compounds and pharmaceutical formulations containing them are also disclosed, as well as methods for the prophylaxis of treatment of a clinical condition using such compounds.
WO2006138510A1 Substituted enaminones as nicotinic acetylcholine receptor modulators The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of α7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on α7 nAChRs in a mammal by administering an effective amount of a compound of Formula (I).
EP2421858A1 Thioxanthene derivatives for the treatment of infectious diseases The present invention is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The invention furthermore relates to compositions comprising said anti-infective agents.
WO2010134614A1 SELF-EMULSIFYING COMPOSITION OF ω3 FATTY ACID A self-emulsifying composition which comprises at least one compound selected from the group consisting of an ω3 polyhydric unsaturated fatty acid and a pharmaceutically acceptable salt and an ester thereof in the total amount of 50 to 95% by mass and an emulsifying agent having a hydrophilic-lipophilic balance of 10 or more in an amount of 5 to 50% by mass, does not need the addition of ethanol or needs the addition of ethanol at a low concentration, has excellent self-emulsifying properties, excellent composition dispersibility, excellent emulsion stability and excellent absorbability, and can be used for medical purposes.
EP1606231A1 Process for preparation of clopidogrel, its salts and pharmaceutical compositions The invention discloses an improved process for racemization of methyl (R)(-) alpha-(2-chlorophenyl)-6,7-dihydro-thieno[3,2-c]pyridine-5(4H)-acetate , a stereoisomer formed in the synthesis of clopidogrel i.e. methyl (S)-(+)-alpha (2-chlorophenyl)-6,7-dihydro-thieno[3,2-c]pyridine-5(4H)-acetate or its salts. The invention is also for an improved process for production of clopidogrel or its pharmaceutically acceptable salts. The invention further discloses novel clopidogrel salts and pharmaceutical compositions comprising them.
CN102898317A Organic amino compounds serving as immunopotentiators, metabolic enhancers or roborants and preparation method and use thereof The invention discloses organic amino compounds serving as immunopotentiators, metabolic enhancers or roborants. The structural formula of the compounds is shown in the description. In the formula, (1) R1 is 2-hydroxypropyl, R2 is ethyl, and R3 is ethyl; (2)R1 is 2-hydroxypropyl, R2 is hydrogen, and R3 is isopropyl; (3) R1 is n-butyl, R2 is methyl or ethyl, and R3 is methyl or ethyl; (4) R1 is n-butyl, R2 is hydrogen, and R3 is isopropyl; (5) R1 is p-hydroxy phenyl ethyl, R2 is methyl or ethyl and R3 or methyl or ethyl; or (6)R1 is p-hydroxy phenyl ethyl, R2 is hydrogen and R3 is propyl. The compounds can increase the immunity in organisms, so that the organisms can resist fermentation with viruses, parasites and bacteria; the compounds can help to treat chronic wasting diseases; the compounds can allow organisms to get strength in time and be more tolerating to resist various irritation; and the compounds can be used as metabolic enhancers, roborants and fat metabolic enhancers to reduce blood fat and help users lose weight.
DE102009014166A1 Product, useful to prevent and treat e.g. acute respiratory diseases such as bronchitis, cough, allergy symptoms and asthma attacks and damages caused by inhalation of atmospheric air pollutants, comprises cobalamin Product comprises cobalamin. - ACTIVITY : Respiratory-Gen.; Cardiovascular-Gen.; Neuroprotective; Antiinflammatory; Antitussive; Antiasthmatic; Antiallergic. - MECHANISM OF ACTION : None given.
WO2008152753A1 Novel crystal of 2-[[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl]-1h-benzimidazole sodium salt and process for producing the same Due to its high tendency of moisture absorption, 2-[[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl]-1H-benzimidazole sodium salt, namely, rabeprazole sodium useful for the treatment of peptic ulcer, etc. has had problems in the storage stability of raw drug and the solid drug formulation. There is provided a novel F-form crystal of rabeprazole sodium free from such problems whose powder X-ray diffraction spectrum has a pattern shown in Fig.1. Further, there is provided a process for producing the F-form crystal, involving crystallizing of rabeprazole sodium from an ether base organic solvent.
US20060063806 4-(4,5,6-trimethoxy-2-benzaldehyde) coumarin; fungicides, nontoxic 4-Substituted coumarin compounds having the general formula of where R is H, CHO, OCH3, X, NO2, an alkyl having C1-10, —OCH2O—, an aryl being mono- or poly-substituted with CN or COOCH3 with the aryl being a phenyl, naphthyl, or azaryl, or a coumarin group that is substituted with R1, R2, R3, R4, with R1, R2, R3, and R4 being H, an alkyl having C1-10, X, NO2, CN, OCH3, COOCH3 or OR5, R5 being H or an alkyl having C1-10, and X being a halogen.
WO2012157672A1 Method for predicting effectiveness of angiogenesis inhibitor The purpose of the present invention is to provide a method for predicting the effectiveness of an angiogenesis inhibitor in a subject affected by a tumor. Provided is a method comprising a step of testing for the presence or absence of an expression deficiency or a mutation in B-Raf and PTEN in a sample of tumor tissue from the subject. By using the presence or absence of an expression deficiency or a mutation in B-Raf and PTEN as an indicator, this method enables the antitumor effectiveness of the angiogenesis inhibitor to be predicted without administering the angiogenesis inhibitor to the subject.
WO2013047373A1 Aqueous formulation containing chlorite The objective of the present invention is to provide a technique that increases the photostability of chlorite contained in an aqueous formulation. By means of the combined use in an aqueous formulation of chlorite and at least one nonsteroidal anti-inflammatory agent selected from the group consisting of bromfenac, diclofenac, ketorolac, flurbiprofen, a pharmaceutically acceptable salt thereof, and nepafenac, it is possible to increase the photostability of chlorite.
US20070232614 Therapeutic Agent for Nonviral Hepatitis The present invention provides a therapeutic drug for non-viral hepatitis, which contains a piperazine compound represented by the following formula (I) or pharmaceutically acceptable salt thereof as an active ingredient.
CN102988963A Clinical research formula of diabetes mellitus The invention relates to a clinical research formula of diabetes mellitus and belongs to the medical field. The clinical research formula is characterized by being prepared by the following materials according to the preparation ratio: 4.85% of calcium, 7.37% of ferrum, 52.7% of enzyme, 17.6% of spirulina, 7% of echinacea and 5.27% of fetal bovine bone marrow, wherein the total content of the six materials is 11392mg.
US20100144852 Bicyclo[2.2.1]hept-7-ylamine Derivatives and Their Uses Compounds of formula (I) have muscarinic M3 receptor modulating activity; Formula (I) wherein A is an oxygen atom or group —N(R12)—; (i) R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group —R5, —Z—Y—R5—Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H; and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a hydrogen atom; or a group —R5, —Z—Y—R5, —Z—NR9R10, —Z—CO—NR9R10, —Z—NR9—CO—R5, or —Z—CO2H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group —Y—R5, —Z—Y—R5, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; R4 is a group of formula (a), (b), (c) or (d); is an C1-C6-alkyl, aryl, aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group, and the remaining variables are as defined in the specification.
WO2014099880A1 Aryl-substituted fused bicyclic pyridazine compounds The present invention provides a compound of formula (I) as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds.
CN102641281A Monosialotetrahexosyl ganglioside sodium for injection and preparation method thereof The invention belongs to the technical field of medicines and specifically relates to monosialotetrahexosyl ganglioside sodium for injection and a preparation method thereof. The monosialotetrahexosyl ganglioside sodium for injection provided in the invention contains GM1, gelatin and PLGA (Polylacticcoglycollic Acid). A microsphere injection prepared from the monosialotetrahexosyl ganglioside sodium for injection provided by the invention is good in reproducibility and encapsulation ratio; the drug-loading rate is improved; the drug release is continuous and stable; the dosage at a time is obviously reduced and the foreign body sensation is reduced; effective blood concentration can be maintained for a long time; the shortcoming of administration every day is avoided; the life quality of a patient is improved; and the problem of the fluctuation of the blood concentration caused by the conventional preparations is solved.
US6855715 Drugs such as 1-(3-Amino-4-chlorobenzoyl-D-phenylglycinyl)-4-(4-fluoro-2 -methylsulphonylphenyl)piperazine, used as anticoagulants Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.
CN1600315A Soft capsule combination of Cloquinate/Promestriene in use for vagina A clothinate/promestriene composition used to prepare the softgel for vagina contains clochinate/promestriene, solvent and surfactant.
CN103113217A Cembrene type diterpene compound, as well as preparation method and application thereof The invention relates to a cembrene type diterpene compound. The technical key points are as follows: the cembrene type diterpene compound is named as (-)-(1S)-15-hydroxy-18-carboxylic cembrene; the molecular formula is C20H30O3; a preparation method comprises extraction and separation; and the cembrene type diterpene compound can be applied to preparation of anti-tumor medicaments. Through a variety of modern spectral analyses, in particular to comprehensive analysis by applying a variety of advanced two-dimensional nuclear magnetic resonance spectra, rotation spectra and other experimental methods, the compound is determined to be a new compound from the aspects of chemical structure and three-dimensional configuration. In-vitro anti-tumor tests prove that the compound has obvious inhibition effect against five tumor cell strains, namely cervical carcinoma (Hela), prostatic carcinoma (PC-3), colorectal carcinoma (HT1080), skin carcinoma (A375-S2) and breast carcinoma (MDA231). The invention provides a lead compound for developing new anti-tumor medicaments and thus has important value for developing and utilizing Beijing spurge root.
CN102824636A Pharmaceutical composition containing statins and polyunsaturated fatty acid and application thereof The invention provides a composition for treating hepatitis b virus infection. The composition contains a treatment effective dose of statins and polyunsaturated fatty acid substances. Excipients permitted in the pharmacy can be added into the composition provided by the invention to prepare a variety of pharmaceutically acceptable medicinal preparations. According to results of research, the composition provided by the invention can substantially reduce secretion of the hepatitis B virus and the level of nucleic acid, has a better effect compared with an individually used component in the composition, has a synergistic effect and can effectively treat diseases like hepatitis, liver cancers and cirrhosis.
CA2319872C Pharmaceutical composition for the treatment of hepatocellular carcinoma The invention mainly discloses a pharmaceutical composition for use in the treatment of hepatocellular carcinoma, which comprises thalidomide and a pharmaceutically acceptable carrier.
WO2013182998A4 Cosmetic and / or pharmaceutical composition for the treatment of skin inflammation and related syndromes The invention relates to a cosmetic and/or pharmaceutical composition in combination with suitable carriers for topical use, comprising a mixture consisting of methyl sulfonyl methane and at least one compound belonging to the class of 4-alkyl cyclohexanols, which is useful in the treatment of various inflammatory conditions such as rosacea. The composition can act to simultaneously hinder both the release of chemical mediators which are up-regulated in rosacea and their action of causing the activation of TRPV receptors. The composition can reduce the effect of ultraviolet radiations on a skin already affected by an inflammatory process, and particularly, it can reduce the erythema induced by ultraviolet radiations on a skin already affected by an inflammatory process.
WO2009144977A1 Oral composition for hair growth Provided is an oral composition for hair growth that has excellent hair growth efficacy, and for which administration or ingestion is not accompanied by severe irritation of the digestive organs. Provided is an oral composition for hair growth that comprises sialic acid and a pharmacologically allowable or edible carrier.
WO2014165070A1 Substituted 2-azabicycles and their use as orexin receptor modulators The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6- membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
EP2199299A2 Antisense modulation of survivin expression Antisense compounds, compositions and methods are provided for modulating the expression of Survivin. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding Survivin. Methods of using these compounds for modulation of Survivin expression and for treatment of diseases associated with expression of Survivin are provided.
US20100104512 Dendritic Chelated Compounds, Methods for Making the Same and Pharmaceutical Compositions Containing the Same The invention relates to dendritic chelated compounds, to methods for producing the same and to pharmaceutical compositions containing the same. The dendritic chelated complexes of the present invention have the following formula (I): [[MC]En-[D]m—X1p1X2p2X3p3X4p4]z − z B+ (I), where m is a magnetic or scintigraphic marker, C is a chelating agent of the marker M, E is a spacer, n=0 or 1, D is compound capable of forming a dendritic structure, m is an integer equal to 1 or 2 or 4, X1 is a group increasing the complex lipophily, p1 is an integer from 0 to 12, X2 is a group increasing the complex specificity for a particular organ, p2 is an integer equal to 1 or 2 or 4, X3 is a group having a therapeutic activity, p3 is an integer equal to 0, 1, 2 or 4, X4 is a CH3 group, p4 is an integer from 0 to 12, B is a counter-ion, z is an integer equal to 0, 1, 2, 3 or 4. The invention can be used in the field of pharmacy, more precisely in medical imaging.
US20110288071 Substituted pyrimidines for the treatment of diseases such as cancer The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
CN100584337C Dispersed tablet of tannic matrine and their preparing method A dispersing tablet of matrine tannate for treating the infantile diarrhea, bacterial dysentery and enteritis is prepared from matrine tannate, polyvinyl pyrrolidone, polyacrylic resin, cross-linked povidone and sweetening agent.
EP1745052B9 Hiv integrase inhibitors: cyclic pyrimidinone compounds The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed. Formula (I).
WO2006042370A1 Hair and nail compositions and methods Methods for maintaining or improving nails and/or hair by administering one or more phytoestrogen isoflavones are described. Also described is the use of one or more of the isoflavones for maintaining or improving hair and/or nail condition and/or strength.
US20060014750 Pharmaceutical compositions for the treatment of CNS and other disorders The present invention relates to a method of treating disorders of the central nervous system (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant α7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant α7 nicotinic receptor agonist.
US20090170807 Methods and means for producing hyaluronan The present invention relates to fungal cells and fungi which synthesize hyaluronan and to methods for preparing such fungi, and also to methods for preparing hyaluronan with the aid of these fungal cells or fungi. Furthermore, the present invention relates to the use of fungi for preparing hyaluronan and to food or feed which comprises hyaluronan.
US7186752 Derivatives of N-(iminomethyl)amines, their preparation, their use as medicaments and the pharmaceutical compositions containing them N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.
WO2013073620A1 Carotenoid-containing composition and method for producing same A carotenoid-containing composition comprising: a carotenoid component that comprises amorphous crystalline carotenoid; a (poly)glycerin fatty acid ester that contains 1 to 6 glycerin units and 1 to 6 fatty acid units and has at least one hydroxy group of a glycerin unit; a fatty acid ester component that is at least one selected from the group consisting of a triester of glycerin and a fatty acid and an ester of an alcohol having one hydroxy group and a fatty acid, has no hydroxy group in the molecule and has 10 to 60 carbon atoms in total; and an antioxidant agent.
CN1569019A Application of arctium fruit glycoside in the preparing process of nephritis treating medicine The invention discloses the application of arctium fruit glycoside in the preparing process of nephritis treating medicine, wherein the arctium fruit glycoside is prepared from the extract of dried great burdock achene fruits, wherein the medicament can be prepared into granule, tablet, or oral form.
US20080242623 Microutrophin and Uses Thereof A microutrophin containing a utrophin having internal deletions (relative to a native utrophin) in the hinge regions and a C-terminal deletion is provided. Also provided are vectors and compositions useful for delivering the microutrophin for the treatment of muscular disorders, including Duchenne Muscular Dystrophy.
WO2006030851A1 Pirenoxine suspension type eye lotion A pirenoxine suspension type eye lotion which is effective in easily dispersing the drug adherent to a container in the liquid. The pirenoxine suspension type eye lotion contains a cellulosic polymer, whereby the drug adherent to a container can be easily dispersed in the liquid. The concentration of the cellulosic polymer is preferably 0.00001-0.1% (w/v). The cellulosic polymer preferably is hydroxypropyl methyl cellulose or methyl cellulose.
WO2012093787A3 Composition for activating gabaa benzodiazepine receptor and composition for anxiety alleviation, convulsion reduction, sedation and sleep induction and improvement containing phloroglucinol, phlorotannin or brown algae extract The present invention relates to a composition for activating a GABAA benzodiazepine receptor containing phloroglucinol, phlorotannin or a brown algae extract as an active ingredient. The brown algae extract has an affinity to a GABAA benzodiazepine receptor, and safety can be obtained without causing side effects because a material obtained from a natural substance is used. Phloroglucinol, phlorotannin or a brown algae extract can be utilized in a pharmaceutical composition for anti-anxiety, anti-convulsion, sedation and insomnia treatment or a food composition for anxiety alleviation, convulsion reduction, and sleep induction and improvement as an active ingredient.
US7244849 Reaction of a phenoxypropionic acid compound with a trifluoromethylphenylthiazole compound; for manufacture of a medicament for treatment of a human peroxisome proliferator activated receptor alpha mediated disease or condition such as hypercholesteremia, cardiovascular disease A method of preparing a compound of formula (I), and pharmaceutically acceptable salts and solvates thereof. Polymorphs of this compound and their use as PPAR ligands are also disclosed
WO2007123186A1 Pharmaceutical product A TLR signaling inhibitor, preferably an inhibitor of the production of various cytokines such as IL-8 or an inflammatory mediator, an inhibitor of the expression of COX-II or the like or an inhibitor of various kinases such as ATF2 containing a compound represented by the formula (I) or the formula (II): (I) (II) (wherein the definition of each symbol is as described in the description), a salt thereof or a prodrug thereof.
CN101664403B Medicinal composition for treating cancer and signal transduction path thereof The invention provides a medicinal composition for treating gynecologic cancer, prostatic cancer, bladder cancer and liver cancer, which contains flavonoids compounds of formula I. The flavonoids compounds have the activities of poisoning cancer cells, and arrest the cancer cells at S and G2/M periods by regulating and controlling cyclin of the cancer cells. Moreover, the flavonoids compounds regulate and control signal transduction paths of caspase-3, PARP, p-38 MAPK, JNK 1/2 and the like to induce the cell apoptosis. The flavonoids compounds can effectively inhibit xenoplastic transplantation cancer cells of naked mice, but have no side effect. The flavonoids compounds and platinum diaminodichloride have cooperative poisoning effect on the cancer cells.
CN102641263A Pharmaceutical composition for inhibiting cancer cell growth A pharmaceutical composition for inhibiting cancer cell growth is used for the inhibition of the growth of androgen-dependent and/or independent prostate cancer cells, liver cancer cells, oral cancer cells, and/or stomach cancer cells, and comprises an effective amount of an active component which is selected from the following groups: compounds shown in formula (I), compounds shown in formula (II), pharmaceutically-acceptable salts and esters thereof, and arbitrary compositions of the above, wherein R is H, alkyloxy, or aryl. Applications of compounds shown in formula (I) and/or compounds shown in formula (II) and/or pharmaceutically-acceptable salts and/or esters thereof in medicament preparation.
WO2013032744A3 Compositions and methods for increasing desirable microbiota A formulation to increase the ratio of gastrointestinal microbiota in phylum Bacteroidetes to microbiota of Firmicutes phylum preferably includes about 20-60 mg/kg of body weight of fermentable fiber, about 10-30 mg/kg of body weight of beta glucan and about 20-60 mg/kg of body weight of blueberry extracts or any fruit or berry ingredient preparation containing similar phenolics. This formulation is preferably used to control body weight, body composition, and blood glucose regulation, preferably in humans, and is preferably administered orally, preferably twice per day.
CN102871962A Drug combination of mezlocillin sodium for injection and preparation method of same The invention discloses a drug combination of mezlocillin sodium, namely mezlocillin sodium nanoparticle injection which comprises mezlocillin sodium, a carrier material, a stabilizing agent and an excipient. The average effective particlesize of nanoparticle is 10 to 20 nm. The preparation method of the injection comprises the steps of mixing the mezlocillin sodium and the stabilizing agent in water for injection, adjusting pH value, and then adding the carrier material and the excipient into the mezlocillin sodium and the stabilizing agent. The mezlocillin sodium nanoparticle injection has the advantages of good re-solubility, good stability, high drug loading capacity and the like, and the method is suitable for industrial production.
CN1883645A Composition for treating acne mainly The invention discloses a group of compositions mainly for treating acne characterized in that,the compositions comprise the active ingredients of Adapalene and/or aloe and/or bee glue. The compositions have synergic and complementary actions of chemical medicaments and plant medicaments.
WO2011006983A1 Amino derivatives of dihydro-1,3,5-triazine for treating oxidative stress The present invention relates to amino derivatives of dihydro-1,3,5-triazine of formula (I), to be used for treating oxidative stress and diseases related thereto, in particular in persons suffering from hyperglycemia.
DE102009052808A1 Ointment, useful e.g. for treating salt deficiency, acute and chronic trauma, comprises ointment base and homeopathically diluted mineral salt including e.g. calcium phosphate, iron phosphate, potassium chloride and potassium phosphate Ointment comprises an ointment base and at least one homeopathically diluted mineral salt including calcium phosphate, iron phosphate, potassium chloride, potassium phosphate, potassium sulfate, magnesium phosphate, sodium chloride, sodium phosphate, sodium sulfate, silica or calcium sulfate. The ointment base contains aqueous vitamin solution comprising vitamin A (0.08-1 mu g), vitamin B1 (0.1-8 mu g), vitamin B2 (0.1-8 mu g), vitamin B3 (0.1-8 mu g), vitamin B5 (0.8-10 mu g), vitamin B6 (0.04-5 mu g), vitamin B12 (0.1-2 ng), vitamin C (5-100 mu g), vitamin D3 (0.1-5 ng) and vitamin E (0.8-10 mu g). Ointment comprises an ointment base and at least one homeopathic diluted mineral salt (0.000001-0.0168%) including calcium phosphate, iron phosphate, potassium chloride, potassium phosphate, potassium sulfate, magnesium phosphate, sodium chloride, sodium phosphate, sodium sulfate, silica or calcium sulfate. The ointment base contains an aqueous vitamin solution (1%) comprising vitamin A (0.08-1 mu g), vitamin B1 (0.1-8 mu g), vitamin B2 (0.1-8 mu g), vitamin B3 (0.1-8 mu g), vitamin B5 (0.8-10 mu g), vitamin B6 (0.04-5 mu g), vitamin B12 (0.1-2 ng), vitamin C (5-100 mu g), vitamin D3 (0.1-5 ng) and vitamin E (0.8-10 mu g). - ACTIVITY : Vulnerary; Antiinflammatory; Dermatological. No biological data given. - MECHANISM OF ACTION : None given.
US20130039927 Antigenic mimics of discontinuous epitopes of pathogen recognized by broadly neutralizing antibodies The present invention relates to an anti-idiotypic polypeptide scaffold that includes two or more peptide sequences that mimic a discontinuous epitope of a pathogen that is recognized by or induces formation of a broadly neutralizing antibody. Using a fibronectin FNfn10 scaffold bearing two or more modified discontinuous loops, scaffolds that recognize broadly neutralizing antibodies in vitro and from patient serum have been identified. These scaffolds should induce an immune response or mobilize germline specificities to initiate their affinity maturation.
CA2486298C Means for weaning people off smoking and alcohol The invention relates to a means for weaning people off smoking or alcohol, said means containing alpha-Ketoglutaric acid and 5-hydroxymethylfurfural, preferably in a mass ratio of between 2:1 and 12:1. Preferably, said means is in the form of a drink containing the following constituents per litre: between 4 and 8g of alpha-Ketoglutaric acid; between 0.2 and 0.6g of 5-hydroxymethylfurfural; between 20 and 40g of saccharose; between 2.5 and 5g of sodium carbonate; between 0.3 and 0.8g of sorbic acid; and optionally up to 0.5g of citric acid. The pH value is equal to between 4 and 5.
CN101590022A Theophylline sodium glycinate slow-release tablet and preparation method thereof The invention provides a theophylline sodium glycinate slow-release tablet and a preparation method thereof. The theophylline sodium glycinate slow-release tablet comprises the following raw materials according to parts by weight: 14-18 parts of theophylline sodium glycinate, 4-7 parts of skeleton material, 5-7 parts of filler, 9-11 parts of adhesive, 0.4-0.6 part of disintegrating agent and 0.07-0.2 part of lubricant; the existing short-acting theophylline sodium glycinate slow-release tablet is prepared into a skeleton type slow-release preparation form, and the skeleton material is a hydrophilic skeleton tablet; after encountering an aqueous medium, colloid at the junction of the tablet and the aqueous medium forms a gel layer because of hydration, and the gel layer controls the release of a medicine, so that the medicine is slowly, durably and stably released, the administration frequency is reduced, and convenience is provided for a patient; especially, the peak time of the blood concentration is shifted so as to achieve the purpose of effectively controlling the nocturnal outbreak of asthma diseases; and the preparation process of the theophylline sodium glycinate slow-release tablet is carried out in a closed one-step boiling granulator, the quality of a finished product can be better guaranteed, and automatic control is convenient.
US20060093665 Method to improve surface properties of pharmaceutical tablets The invention provides a method to improve surface properties of tablets having a matrix consisting of at least 55% of a cellulose ether, characterised in that the method comprises briefly exposing the tablets to a hydrous solvent.
EP1603566B1 Use of isoquinoline derivatives for treating cancer and map kinase related diseases This invention relates to the treatment of a disease that is characterized by an aberrant MAP kinase signaling pathway by administering a compound of the formula (I) wherein the variable substituents are defined herein, to a patient in need of such treatment. The inventive method is especially useful for the treatment of cancers that have a mutated RAF kinase, especially melanoma.
WO2011149354A1 Mirnas involved in the blood brain barrier function The current invention relates to use of particular nucleic acids for modulating (increasing or decreasing) blood-brain barrier function, and for use of such nucleic acids in treatment of conditions involving blood brain barrier function, including multiple sclerosis, HIV infection, Alzheimer's disease, Parkinson's disease, epilepsy, and so on. Also provided is an assay for identifying drugs useful in modulating blood brain barrier function.
US6900242 Compound for use in the treatment of cancer and prevention of infections Compounds of Formula Ia and Ic having a lactone structure and an methylene group at the alpha-position of the lactone structure and methods for using and making the compounds have been disclosed. The lactone compounds can be reacted with an neucleaphilic agent to open the lactone ring to a compound of Formula Ib. The lactone of Formula Ia and its functional derivatives have been isolated from Securidaca virgata. These compounds are referred to as LMSV-6 or Securolide™. The purified compounds have demonstrated activity in assays for anti-bacterial and anti-fungal activities, and for treating proliferation disorders such as cancer. Based on the in vitro assays, the lactones are useful for treating proliferation disorders including, for example, breast cancer, colon cancer, rectal cancer, stomach cancer, pancreatic cancer, lung cancer, liver cancer, ovarian cancer, esophageal cancer, and leukemia. They are also effective for treatment of bacterial and fungal infections, including treatment of peptic ulcer disease, gingivitis and periodontitis. The lactone and its derivatives has the following chemical structure: wherein R1-R9 and Y1-Y3 taken independently are preferably a hydrogen atom, a halogen atom, a hydroxyl group, or any other organic groups or groupings which optionally include a heteroatom such as oxygen, sulfur, or nitrogen groupings in linear, branched, or cyclic structural formats; Z and X are independently and preferably a heteroatom such as oxygen, sulfur, or nitrogen groupings in linear, branched, or cyclic structural formats; and Z′ may a hydrogen atom, a halogen atom, a hydroxyl group, or any other organic groups or groupings which optionally include a heteroatom such as oxygen, sulfur, or nitrogen groupings in linear, branched, or cyclic structural formats.
CA2728096A1 Compound with serotoninergic activity, process for preparing it and pharmaceutical composition comprising it Compound of formula (I) in which R1, R2 and R3 are defined in the following description, and the pharmaceutically acceptable acid-addition or base-addition salts thereof. The invention also relates to a process and an intermediate for prepar-ing it, and to a pharmaceutical composition comprising it. The invention also relates to the use of a novel 2H-pyrrolo[3,4-c]quinoline compound for preparing a pharmaceutical composition that is active in the treatment of disturbances of the serotoninergic system.
US20100292311 Oligomeric compounds for the modulation of survivin expression Oligonucleotides directed against the survivin gene are provided for modulating the expression of survivin. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the survivin. Methods of using these compounds for modulation of survivin expression and for the treatment of diseases associated with either overexpression of survivin, expression of mutated survivin or both are provided. Examples of diseases are cancer such as lung, breast, colon, prostate, pancreas, lung, liver, thyroid, kidney, brain, testes, stomach, intestine, bowel, spinal cord, sinuses, bladder, urinary tract or ovaries cancers. The oligonucleotides may be composed of deoxyribonucleosides or a nucleic acid analogue such as for example locked nucleic acid or a combination thereof.
US20100197622 Non-Peptide Macrocyclic Histone Deacetylase (HDAC) Inhibitors and Methods of Making and Using Thereof Compounds of Formula I or II, and methods of making and using thereof, are described herein. M represents a macrolide subunit, n is a C1-6 group, optionally containing one or more heteroatoms, D is an alkyl or aryl group, A is a linking group connected to D, B is an alkyl, alkylaryl or alkylheteroaryl spacer group, ZBG is a Zinc Binding Group, R1, R2 and R4 are independently are selected from hydrogen, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 alkanoate group, a C2-6 carbamate group, a C2-6 carbonate group, a C2-6 carbamate group, or a C2-6 thiocarbamate group, R3 is hydrogen or —OR5, R5 is selected from a group consisting of Hydrogen, a C1-6 alkyl hgroup, a C2-6 alkenyl group, a C2-6 alkynyl group, C1-6 alkanoate group, C2-6 carbamate group, C2-6 carbonate group, C2-6 carbamate group, or C2-6 thiocarbamate group.
EP2402033A1 Cell adhesion inhibitor and use thereof Disclosed is a means for preventing or treating cancer through the regulation of the expression or function of a target molecule that is different from those utilized in conventional techniques, as a novel means to be used in a molecule targeting therapy for cancer. Also disclosed is a means for screening a substance having a prophylactic or therapeutic activity on cancer using the target molecule. Specifically disclosed is a cell adhesion inhibitor for a cancer cell, which comprises an antibody directed against a protein comprising an amino acid sequence that is identical or substantially identical to the amino acid sequence depicted in SEQ ID NO:2, SEQ ID NO:4 or SEQ ID NO:6 or a partial peptide of the protein. Also disclosed is a cell adhesion inhibitor for a cancer cell, which comprises an antisense polynucleotide comprising a nucleotide sequence or a part thereof, wherein the nucleotide sequence is complementary or substantially complementary to a nucleotide sequence for a polynucleotide encoding a protein comprising an amino acid sequence that is identical or substantially identical to the amino acid sequence depicted in SEQ ID NO:2, SEQ ID NO:4 or SEQ ID NO:6. Further disclosed is a cell adhesion inhibitor for a cancer cell, which comprises a substance capable of inhibiting the expression and/or activity of a protein comprising an amino acid sequence that is identical or substantially identical to the amino acid sequence depicted in SEQ ID NO:2, SEQ ID NO:4 or SEQ ID NO:6
EP2772490A1 Aminoalkyl-substituted n-thienyl benzamide derivative [Problem] To provide a compound that has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. [Means for Solution] The present inventors conducted thier studies on a compound that has an NPT-IIb inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. As a result, they created an aminoalkyl-substituted N-thienylbenzamide derivative which has NPT-IIb inhibitory action, thereby completing the present invention. The aminoalkyl-substituted N-thienylbenzamide derivative of the present invention has an NPT-IIb inhibitory action and can be used as an agent for preventing and/or treating hyperphosphatemia.
WO2009124024A1 Compositions and methods for inhibition of hepatocyte growth factor receptor c-met signaling Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met obtained by virtual screening, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives.and analogs of c-Met inhibitors and methods of use thereof are provided. Formula (I)
US20130053393 Methods and compositions for treating peripheral vascular disease The invention features a method of treating a peripheral vascular disease or a condition associated with a peripheral vascular disease by administering to a subject an effective amount of at least one phosphodiesterase type 5 inhibitor and at least one nitric oxide donor. The invention also features compositions formulated for topical or oral administration including at least one phosphodiesterase type 5 inhibitor, at least one nitric oxide donor, and a pharmaceutically acceptable carrier, as well as kits including these compositions. These methods, compositions, and kits can optionally include other therapeutic agents.
US20120021021 Method for preparing pharmaceutical compositions comprising fine particles of active substance The present invention relates to a method for preparing solid pharmaceutical compositions comprising fine particles of at least one active substance, dispersed on and (or) within a divided solid. This method is characterized in that a solution is formed which comprises at least one active substance in a fluid at supercritical pressure, said solution then being expanded in a chamber under temperature and pressure conditions for which a part of said fluid is in the liquid state at the time of the expansion, said fluid thus expanded being brought into contact with a divided solid in said chamber.
US20140004113 Defensin-antigen fusion proteins The present invention relates to a vaccine for increasing the immunogenicity of a tumor antigen thus allowing treatment of cancer, as well as a vaccine that increases the immunogenicity of a viral antigen, thus allowing treatment of viral infection, including immunodeficiency virus (HIV) infection. In particular, the present invention provides a fusion protein comprising a defensin fused to either a tumor antigen or viral antigen which is administered as either a protein or nucleic acid vaccine to elicit an immune response effective in treating cancer or effective in treating or preventing viral infection.
US7163961 useful in preventing or treating diseases accompanied by a decrease in bone weight and hypertension or diseases resulting from hypertension The present invention provides a composition for preventing or treating diseases accompanied by a decrease in bone weight, hypertension and diseases resulting from hypertension, the composition containing, as an active component, at least one member selected from the a compound represented by formula (I) wherein A and B are the same or different and are independently selected from the group consisting of halogen, amino, amidino, anilinoamide, mercapto, sulfonic acid, phosphate, carboxy, hydroxy C1–C5 alkyl, sugar residue, —OR1, and —OCOR2; wherein R1 is selected from the group consisting of hydrogen, C1–C5 alkyl, hydroxy C1–C5 alkyl, and C2–C5 alkenyl; and R2 is selected from the group consisting of C1–C5 alkyl, hydroxy C1–C5 alkyl, and C2–C5 alkenyl; n is number of substituents A present and is a number from 0 to 5; and m is number of substituents B present and is a number from 0 to 5.
US8288442 Use of derivatives of valproic acid amides and 2-valproenic acid amides for the treatment or prevention of pain and/or headache disorders A method for the treatment or prevention of pain and/or a headache disorder using a derivative of a valproic acid amide or a 2-valproenic acid amide, as well as pharmaceutical compositions comprising these derivatives or compounds.
US20110044904 Crystal forms of 2--adenosine The present invention provides novel crystalline polymorphic forms of 2-cyclohexylmethylidenehydrazino adenosine, also known as binodenoson, methods of making the same, and methods for the manufacture of a pharmaceutical composition by employing such crystal forms, in particular, for the use of binodenoson in a subject, in need thereof, as a pharmacological stress agent to produce coronary vasodilation.
US20110257238 Heteroaryl Dihydroindolones as Kinase Inhibitors The present invention provides a compound represented by the formula: wherein the variables R1, b, R6, Y, Z, X, R and a are defined in the specification. Said compound may be used in a method for treating diseases related to unregulated tyrosine kinase signal transduction, wherein said disease is selected from the group consisting of cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, and metabolic diseases.
CN1594587A Preparation for fungus extracellular polysaccharide compound and application thereof The invention concerns biological pharmacy field. Extracellular polysaccharides compound is extracted from Chinese caterpillar fungus -Tolypocladium sinense culture liquor. The sugar content of extracellular polysaccharides compound is 65í½80úÑ, while protein content is 6í½9úÑ. Extracellular polysaccharides compound has good effect on suppressing tumor grow and transfer, can also promote body immunity, and prepare anti tumor drug and healthcare food. The extracellular polysaccharides compound has low price, easy to produce, stable in curative effect, safe.
WO2004032843A3 Mucoadhesive tetracycline formulations Mucositis is treated and/or prevented by administrating to a patient a formulation containing a tetracycline and at least one cationic polymer and/or mucoadhesive material. The tetracycline may be in the form of a pharmaceutically acceptable salt or a base. The formulations may optionally also contain an antifungal agent to prevent fungal overgrowth due to reduction in the normal oral flora by the tetracycline. The formulation can be formed into liquid or solid dosage forms such as mouth rinse or tablet. Such compositions have the advantage of prolonged retention of the tetracycline in the mucosa of the oral cavity.
CN102018710A Composition for treating erectile dysfunction and/or for alleviating fatigue The invention relates to a composition for treating erectile dysfunction and/or for alleviating fatigue, which comprises propionyl L-Carnitine, arginine and niacin. The composition further comprises acetyl-L-Carnitine, vitamin E, glycocoll, vitamin C, beita-carotene, vitamin B6, one or more elements of potassium, magnesium and zinc. The invention also relates to the application of the composition to medicines and food for curing erectile dysfunction and/or for alleviating fatigue.
WO2009052071A1 Treatment of sensorimotor disorders with 4- ( 1- ( 2, 3 -dimethylphenyl) ethyl) -1h-imidaz0le-2 ( 3h) -thione Disclosed herein is a method of treating sensorimotor disorders comprising administering to a subject in need of such treatment 4-(1-(2,3- dimethyiphenyl)ethyl)-1 H-imidazole-2(3H)-thione.
WO2014017643A1 Difluoromethylene compound The present invention relates to: a compound which has URAT1 inhibitory activity; and a URAT1 inhibitor, a blood uric acid level reducing agent and a pharmaceutical composition, each of which contains the compound. The present invention more specifically relates to a compound represented by formula (I). (In the formula, R1 represents -Q1-A1 or the like; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group or the like; each of W1, W2, W3 and W4 independently represents a nitrogen atom, an optionally substituted methine group or the like; each of X and Y represents a single bond, an oxygen atom or the like; and Z represents a hydroxyl group, COOR3 or the like.)
EP2277878A1 Process for production of ethynylthymidine compound using 5-methyluridine as starting raw material The present invention provides a process for producing 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, which is useful as a medicine, in an efficient and industrially advantageous manner, and more specifically, provides a process for producing 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine as shown below. (wherein R1 and R2 independently represent a protective group for a hydroxy group, or R1 and R2 together form a protective group for two hydroxy groups, R3 and R4 independently represent a protective group for a hydroxy group, R5 represents a protective group for a hydroxy group, R6 represents a protective group for a hydroxy group, X represents a leaving group, and Y represents a halogen atom.)
EP0882065B1 Novel human metabotropic glutamate receptor A novel human metabotropic glutamate receptor (mGluR) protein is identified, sequenced, and cloned. The receptor may be used to screen for compounds that modulate the activity of the mGluR. The recombinant mGluR as well as compounds that modulate mGluR activity may be used in the diagnosis and treatment of neurological disorders and diseases.
CN1628695A Eye lotion containing hyaluronic acid and hyaluronic salt and method for making same The invention provides an eye lotion containing hyaluronic acid and hyaluronic salt and method for preparation, wherein the lotion comprises lubrication humectant, inorganic salt, antiseptic germicide, vitamins, vasoconstrictor, antiallergic and algefacient. The lotion is used for washing eyes or eyeball surface.
US20120064178 Cell-8 Solution Cell-8 Solution is an intravenous solution introduced into the veins of the patient. Cell-8 Solution provides the cells of the body with highly absorbed minerals as well as new RNA information which changes the relationship of the body to the cancer in question. Treatment with Cell-8 Solution will prevent the body from accepting the existence of cancer cells so that cancer cell replication will no longer occur. Although intravenous Cell-8 Solution is superior, other applications include nebulized, transdermal and oral.
WO2008134630A1 Dexrazoxane compounds for cardioprotection Methods are disclosed of treating conditions associated with iron and calcium overload comprising administering an effective amount of dexrazoxane or a non- dexrazoxane compound of formula (IA), (IB), or (IC) or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof.
EP1753724A1 Heterocyclic derivatives for treatment of hyperlipidemia and related diseases The present invention provides compositions adapted to enhance reverse cholesterol transport in mammals. The compositions are suitable for oral delivery and useful in the treatment and/or prevention of hypercholesterolemia, atherosclerosis and associated cardiovascular diseases.
WO2008138483A1 sGC STIMULATORS, sGC ACTIVATORS AND COMBINATIONS FOR THE TREATMENT OF UROLOGICAL DISORDERS The invention provides pharmacological compositions comprising a stimulator or activator of the soluble guanylate cyclase alone (sGC) or in combination with a PDE5 inhibitor for the treatment of urological disorders comprising of Benign Prostate Syndrome (BPS), Benign Prostate Hyperplasia (BPH), Benign Prostate Enlargement (BPE), Bladder Outlet Obstruction (BOO), Lower Urinary Tract Symptoms (LUTS), genitourinary disorders comprising neurogenic bladder syndrome (OAB) and (IC), urinary incontinence (UI) like mixed-, urge-, stress-, or overflow incontinence (MUI, UUI, SUI, OUI) and pelvic pain (PP).
US7459430 Calcium channel modulator; delayed or sustained release The invention relates to methods of using Cav2.2 subunit calcium channel modulators to treat painful and non-painful lower urinary tract disorders and the related genitourinary tract disorders vulvodynia and vulvar vestibulitis in normal and spinal cord injured patients.
CN102526492A Medicament for treating burn and scald and preparation method thereof The invention discloses a medicament for treating burn and scald and a preparation method thereof. The medicament is prepared from astragalus, coptis root, amur corktree bark, garden burnet root, toad, asparagus, pollen, common andrographis herb, sinkiang arnebia root, safflower, frankincense, myrrh, rehmannia root, common threewingnut root, pseudo-ginseng, cockscomb flower, tree peony root-bark, giant knotweed, common bletilla tuber, honeysuckle flower, catechu, moschus, Vaseline and chitin, can be used for effectively curing burn and scald caused by water, fire, acid and the like, and has the advantages of high recovering speed, good curative effect and freeness from scar.
CN102329284A Compound as well as preparation and application thereof The invention belongs to the technical field of medicines and discloses a new compound (3S, 9R, 10R)-9,20-epoxy-1-heptadecene-4,6-diyne-3-alcohol. A pharmacological test shows that the compound disclosed by the invention has a better anticancer activity. The invention also discloses a synthesis method of the compound, and the synthesis method has the advantages of fewer reaction steps, mild reaction conditions, high yield, good stereoselectivity and the like.
CN1850123A Method for preparing humanbody nutritious intensifier preparation by using winter mushroom and use The present invention relates to a nutrient-enriching substance for human body. Said nutrients-enriching substance mainly contains 40-85% (V/V) of long rooted mushroom extract, 1-5.0% (W/V) of taurine, 1-5.0% (W/V) of glutaminate, 1-5.0% (W/V) of honey and the rest excipient. It can promote intelligence development of small fry and raise immunity of body.
WO2013006308A3 Dihydropyrazoles, pharmaceutical compositions thereof and their use for the treatment of fertility disorders Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
CN103476765A Method of inhibiting hamartoma tumor cells Dimorpholinopyrimidines are useful for inhibiting growth or proliferation of hamartoma tumor cells. Because the Dimorpholinopyrimidines inhibit the growth and proliferation of hamartoma tumor cells they are also useful in treating PTEN hamartoma tumor syndromes. The therapeutic and prophylactic treatments provided by this invention are practiced by administering to a patient in need thereof an amount of a compound of dimorpholinopyrimidine derivative that is effective to inhibit growth or proliferation of the hamartoma tumor cells.
CN103690474A Method for preparing ibuprofen cream The invention discloses a method for preparing ibuprofen cream. The method comprises the following steps: mixing white vaseline, lanolin, beewax and menthol and dissolving to obtain an oil phase; dissolving carboxymethyl-ethyl-beta-cyclodextrin in water to obtain carboxymethyl-ethyl-beta-cyclodextrin solution, dissolving ibuprofen in ethyl acetate to obtain an ibuprofen ethyl acetate solution; adding the ibuprofen ethyl acetate solution into the carboxymethyl-ethyl-beta-cyclodextrin solution to prepare an ibuprofen cyclodextrin inclusion solution, adding ethyl p-hydroxybenzoate into the ibuprofen cyclodextrin inclusion solution to obtain a water phase; adding the oil phase into the water phase, stirring to prepare the ibuprofen cream, and flavoring and filling. By virtue of the ibuprofen cream prepared by the method, the infiltration speed of the ibuprofen cream can be improved, so that the characteristics of quick acting and good pain relieving effect can be achieved.
CN101724054A Human epididymal expression sperm binding protein HEL-213 as well as encoding gene and application thereof The invention belongs to the biotechnology and the medical field and discloses a new human epididymal specific expression sperm binding protein HEL-213 as well as preparation and application thereof. The invention discloses an amino acid sequence of the HEL-213 protein and provides a recombinant expression vector which carries a DNA sequence used for encoding the protein. The protein is located in an acrosomal region of a mature sperm, has higher expression level in the head and the body of an epididymis, a testis, a heart, a liver, a spleen and a kidney and has no expression in a stomach tissue. A band of about 20 KD is detected in the epididymis by using Western blot. The HEL-213 protein can be used as a target protein for developing an immunological contraceptive and clinically diagnosing and treating male infertility. A method for detecting a corresponding gene or protein based on development of the HEL-213 protein can be widely used for the research field of reproductive medicine.
US20120213736 Parvovirus methods and compositions for killing neoplastic cells According to the invention, parvoviruses such as the adeno-associated virus Type 2 (AAV2) are found to be oncolytic, selectively mediating apoptosis in cancer cells and their precursors, while leaving healthy cells intact. The invention also includes a method of killing cancer and other neoplastic and preneoplastic cells by administrating to said cells the AAV2 proteins Rep78 or Rep 68, expression constucts encoding the same, or pharmaceutical compositions comprising the same.
US8778876 Small-molecule inhibitors of Dengue and West Nile virus proteases The present invention concerns methods and compositions involving small molecule inhibitors for the treatment or prophylaxis of flavivirus infection, such as dengue virus and West Nile virus.
WO2008117225A3 New imidazolo-heteroaryl derivatives with antibacterial properties The invention relates to Imidazolo-heteroaryl derivatives of formula (I). The compounds inhibit the activity of the Dlta enzyme of Gram-positive bacteria and are useful to treat Gram-positive bacterial infections. Furthermore the application discloses method for assessing the Dlta inhibitory activity of tested molecules and a method for measuring the efficacy of molecules in inhibiting bacteria proliferation in vitro.
US20120015039 Sustained release of nutrients in vivo Nutritional compositions delivered in vivo in a time controlled manner sustainable over long periods of time, provide enhancing athletic performance, increased hand/eye coordination and concentration on the task at hand.
US7732414 cosmetic make-up removing composition; for treating aging, fibroblasts, keratinocytes; particularly hyaluronic acid, proteoglycans C-glycoside compounds are suited for stimulating the synthesis of glycosaminoglycans containing a D-glucosamine and/or N-acetyl-D-glucosamine residue, advantageously hyaluronic acid, and/or proteoglycans, advantageously proteoglycans containing hyaluronic acid, by fibroblasts and/or keratinocytes.
US20060019970 Methods and compositions for the treatment of neuroleptic and related disorders using ziprasidone metabolites The invention relates to novel methods using, and pharmaceutical compositions comprising, ziprasidone metabolites. The methods and compositions of the invention are suitable for the treatment of neuroleptic and related disorders. The invention further encompasses methods of preparing ziprasidone sulfoxide and ziprasidone sulfone.
WO2014049297A1 Combination of laropiprant and oxymetazoline for the treatment of rosacea The invention relates to a pharmaceutical composition, in particular a dermatological composition, comprising laropiprant, an ester or a pharmaceutically acceptable salt thereof and oxymetazoline or a pharmaceutically acceptable salt thereof, and to the use of same for the treatment of dermatological conditions, in particular rosacea.
WO2014078447A1 Calcium flux agonists and methods therefor Calcium flux agonists are used to enhance a TLR- or NOD-mediated stimulus and to so increase an immune response of a host and reduce healing time. Preferred calcium flux agonists include Ca2+ ionophores and SERCA inhibitors and are used in synergistic quantities where a ligand to a TLR or NOD receptor is present.
EP1545592A1 Combination treatment of cancer using a cancer vaccine and a chemotherapeutic drug The invention is a method of treating a patient suffering from cancer. In the method, an agent for stimulating an immune response against the cancer and a chemotherapeutic drug are administered to the patient. The drug is administered in a metronomic scheduble to prevent it suppressing immune response and the effectiveness of the agent for stimulating an immune response against the cancer.
US7396834 e.g., 3-[(4-[(diethylamino)carbonyl]phenyl)(4-benzyl-piperazin-1-yl)methyl]benzamide; opioid delta rreceptor agonist; analgesic, hypotensive agent; pain, anxiety and functional gastrointestinal disorders, immunomodulatory activities Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
WO2012005339A1 Prophylactic or therapeutic agent for diabetes A prophylactic or therapeutic agent for diabetes, which comprises a polynucleotide such as miR-199b*; a method for screening for a prophylactic or therapeutic agent for diabetes, which comprises measuring the expression amount of a polynucleotide such as miR-199b*; and a method for determining the sensitivity to a prophylactic or therapeutic agent for diabetes, which comprises measuring the expression amount of a polynucleotide such as miR-199b*.
WO2014151863A1 Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer The present invention provides MDM2 inhibitor compounds of Formula (I), or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor of Formula (I).
EP1030567B1 System for dialysis and shock treatment A dialysis system (10) and method for removing toxic matter from the large intestine includes an input tube (22), an ouput tube (24) concentric with the input tube (22), both of which tubes (22, 24) are to be inserted in the large intestine, an input pressure pump (12) connected to the input tube (22) to deliver filtrate solution from an input container (14) and an output suction pump (30) connected to the output tube (24) to remove filtrate solution. Pressure gauges control the input and output pumps (12, 30). A filtrate solution composition includes a vasodilator of niacin, a high molecular weight protein in the form of casein, a mineral constituents and other components is also provided. The system and method may be adapted to treat shock. A shock treatment composition may comprise electrolytes, buffers and a rehydrating agent.
US20080233151 Calmodulin and metalloproteinase exotoxins; vaccine; anthrax The invention relates to methods for protecting and/or treating a mammal at risk of acquiring a condition associated with bacteria that produce a calmodulin exotoxin, a metalloproteinase exotoxin, or both, by administering a non-antibacterial tetracycline formulation.
US7850968 Cluster of differentiation 83 specific immunoglobulin for use in treatment of autoimmune and neoplastic disorders The invention provides methods for modulating cytokine levels, GM-CSF levels and the immune system using CD83 nucleic acids, CD83 polypeptides, anti-CD83 antibodies and factors that influence CD83 activity or expression. The invention also provides mice having a mutant CD83 gene and mice having a transgenic CD83 gene, which are useful for defining the role of CD83 in the immune system and for identifying compounds that can modulate CD83 and the immune system.
CN101780266A Compound preparation for preventing and treating respiratory disease of livestock and poultry The invention relates to a compound preparation for preventing and treating respiratory diseases of livestock and poultry, which is characterized by being prepared by uniformly mixing the following components by taking 100 grams as unit weight: 2-5 grams of cefixime sodium, 10-30 grams of doxycycline hydrochloride, 5-10 grams of rifampicin, 5-20 grams of cimetidine, 2-10 grams of ndometacin sodium, 2-6 grams of propolis powder, 2-6 grams of muramyl dipeptide and the balance of pharmaceutically applicable auxiliary materials, wherein the pharmaceutically applicable auxiliary materials are anhydrous glucose or oral glucose, preferably the anhydrous glucose. The compound preparation is compounded by antibiotic drugs, antiviral drugs, immunopotentiator and mucosa repair factors and has efficient and fast cure effect on respiratory symptoms of the livestock and the poultry, easy preparation, obvious effect and wide application range.
CN103608011A Methods and compositions suitable for preventing and treating hyperleptinemia The invention provides methods and compositions suitable for preventing and treating hyperleptinemia, preventing and treating insulin resistance, preventing and treating cardiovascular disease, preventing and treating obesity, preventing and treating hyperlipidemia, and preventing and treating hypertension in an animal. The methods comprise administering one or more isoflavones to the animal, preferably in amounts of from about 0.001 to about 10 g/kg/day.
WO2013122778A1 Methods of treating and preventing diseases and disorders of the central nervous system Disclosed is a method of treating or preventing a disease or disorder of the central nervous system (CNS) in a patient comprising administering transcranially, for example, directly to the skull, an effective amount of an anti-inflammatory agent to the patient. Examples of the anti-inflammatory agent include glutathione and inhibitors of purinergic receptors such as P2X4,P2X7, P2Y6, and P2Y12receptors. Examples of disease or disorder of the CNS include brain injury, particularly traumatic brain injury, inflammation, infection, degeneration of brain cells, stroke, brain edema, tumor, Alzheimer's disease, Parkinson's disease, and multiple sclerosis. Also disclosed is a kit comprising at least one anti-inflammatory agent and printed materials containing instructions for transcranially administering the anti-inflammatory agent to the patient having a disease or disorder of the CNS. isorder of the CNS.
WO2011067571A1 Co - crystals of a triazolo [4,5 - d] pyrimidine platelet aggregation inhibitor The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4- hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2- methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).
WO2014026372A1 Pharmaceutical composition for inhibiting autophagy of motor neurons and use thereof Disclosed is a pharmaceutical composition for inhibiting autophagy of motor neurons containing an effective amount of an active ingredient. The active ingredient is selected from the following groups: a compound of formula (I), pharmaceutically acceptable salts thereof, pharmaceutically acceptable esters thereof and a combination of the foregoing, wherein A is C1-C5 hydrocarbyl with one or more unsaturated bond as needed and is substituted by one or more substituent selected from the following groups as needed: -OΗ, =O, and C1-C3 hydrocarbyl; X is Η, -OΗ, formula (II) or formula (III); Y is O or S, and can form a five-membered ring by binding with A as needed; and R1 is H or a substituted or unsubstituted C1-C20 hydrocarbyl, wherein one or more -CH2- of the hydrocarbyl is replaced by -NH- or -O- as needed.
CN102885835A Application of Gypensapogenin B in medicament for treating yellow fever virus infection The invention discloses an application of Gypensapogenin B in the preparation of a medicament for treating or preventing yellow fever virus infection. Gypensapogenin B is capable of efficiently inhibiting the propagation of yellow fever virus, but has little toxicity for cells; and Gypensapogenin B is further capable of developing the medicament for treating diseases caused by these viruses, and has wide application prospect. The application of Gypensapogenin B in the preparation of the medicament for treating yellow fever virus infection is firstly disclosed; since the skeleton type belongs to an entirely new skeleton type and the inhibition for yellow fever virus activity is previously unimagined high without any possibility of giving out revelation by other compounds, the application has outstanding substantial characteristics; and simultaneously, the application for preventing and treating yellow fever virus infection is obviously advanced.
CA2535516A1 Silencing of tgf-beta receptor type ii expression by sirna The present application is directed to siRNA-based silencing of the type II receptor of TGF.beta.. siRNAs that target this receptor abrogate the receptor protein and transcript, TGF.beta.-mediated processes such as fibronectin assembly and cell migration also are inhibited and the molecules of the invention are efficacious in reducing the inflammatory response and matrix deposition. These findings show that siRNAs can be successfully delivered both in vitro and in vivo to regulate the TGF.beta. type II receptor level and modulate wound response. Methods and compositions exploiting the findings of the present invention have a wide-ranging application, extending from treatment of disorders of the eye to other organs and tissues throughout the body.
US20100074889 4'-allene-substituted nucleoside derivatives The present invention discloses compounds of formula (I), or its β-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof: which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral/anti-proliferative compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral infection in a subject in need of such therapy with said compounds.
US8158158 Composite biocidal particles A biocidal composition is disclosed comprising composite particles, each of said composite particles containing a shell and a core, said core comprising a metal or a metal-containing compound wherein the metal is a moiety selected from the group consisting of zinc, copper, bismuth, silver, zirconium, and combinations thereof said shell comprising a pyrithione adduct comprising the reaction product of pyrithione with a portion of said core metal or metal compound. In one aspect, an anti-fouling composition is disclosed comprising (a) an anti-soft-fouling effective amount of copper pyrithione; and (b) an anti-hard-fouling effective amount of a copper-containing salt, or oxide or hydroxide thereof. The present invention also relates to a method of making an anti-fouling composition comprising particles of copper pyrithione and a copper-containing salt that is effective against hard-fouling and soft-fouling organisms.
WO2006045156A1 Therapy for multi-drug resistant microorganisms A pharmaceutical or veterinary composition comprising an antimicrobial peptide and a macrolide component together with a pharmaceutically or veterinarily acceptable carrier, wherein said antimicrobial peptide and macrolide component interact synergistically against a multi-drug resistant microorganism, a method of treatment and/or prophylaxis of an infection caused by a multi-drug resistant microorganism using said composition in the manufacture of a medicament for said treatment.
EP2671888A1 3',5'-cyclic nucleoside phosphate analogues A compound or salt thereof having the following structure useful for the treatment of hepatitis C virus (HCV): wherein R7 is C1-6 alkyl or C3-6 cycloalkyl and R8 is -O(C1-6 alkyl) or -O(C3-6 cycloalkyl).
CN1582942A Compoiste preparation of cefuoxime sodium A composite cefuroxime sodium is prepared from cefuroxime sodium or its salt and beta-lactamase inhibitor in weight ratio of (4-8):1.
US20100075997 Use of pkc inhibitors in transplantation The present invention pertains to the use of a PKC inhibitor in the treatment of insulin-producing cell and tissue rejection, such as islet transplantation rejection or rejection of transdifferentiated insulin-producing hepatocytes.
CN101428124B Preparation method of plaster for strongly improving phylactic power The invention provides a method for preparing a plaster for improving immunity, which is characterized by firstly dipping the main medicine by a cooked oil, frying, then naturally cooling, and filtering to remove the drug dregs, fully mixing with yellow lead and adding water for dipping; grinding a first part of adjuvant herb into powder for standby; grinding a second part of the adjuvant herb into powder for standby; adding a third part of the adjuvant herb into water and decocting by using slow fire, condensing the obtained drug soup and adding the soup into the second part powder of the adjuvant herb and uniformly stirring, drying and grinding into powder for standby; heating the ointment, then uniformly mixing with the first part powder, the dried grinded powder according to a ratio, then obtaining the immunity plaster. The main medicine and the adjuvant herb comprise the following components by weight: the main medicines comprise golden thread, baical skullcap root, dried ginger, amur corktree bark, prepared common monkshood daughter root and pepper with 50-75g for each, the adjuvant herb comprise three parts, the first part comprises flos caryophyllata and borneol with 30g-50g for each, the second part comprises frankincense, myrrh, flos caryophyllata, prepared Sichuan pepper, villous amomum fruit, immature bitter orange and green tangerine peel with 70-100g for each and the third part comprises sal ammoniac and Chinese asafoetida with 100g-130g for each.
CN102228470B Preparation method and purpose of copper-loaded chitosan antiseptic The invention discloses a preparation method of a copper-loaded chitosan antiseptic, comprising the following steps: 1) adding chitosan into an acid solution with a mass concentration of 0.1 to 5% so as to obtain a chitosan acid solution; 2) adjusting the pH value of the chitosan acid solution to be 3 to 5, thereby forming corpuscule emulsion; 3) centrifuging the corpuscule emulsion to obtain corpuscules, adding corpuscules into a copper salt solution, adjusting the pH value of the solution to be 4.5 to 5.5, and standing the mixture for reaction at room temperature for 5 to 10 hours so as to obtain emulsion; 4) adjusting the pH value of the emulsion to be 7 to 9, carrying out rinsing 3 to 7 times, carrying out refiltering or centrifuge dewatering, and collecting solid products; 5) crushing the solid products after drying so as to obtain the copper-loaded chitosan antiseptic. The purpose of the copper-loaded chitosan antiseptic is to use the antiseptic as a feed additive for aquatic livestock.
US7470430 Modifications of HIV, ENV, GAG, and POL enhance immunogenicity for genetic immunization Modified HIV Env, Gag, Pol, or Nef DNA with improved ability to elicit antibody and CTL responses to HIV antigens have been identified as prototype immunogens for the treatment and prevention of HIV infections. Modifications to Env glycoprotein include deletions in the cleavage site, fusogenic domain, and spacing of heptad repeats 1 and 2 and different COOH-terminal deletions. Other modifications entail expression of Gag-Pol and Gag-Pol-Nef as fusion proteins.
CN1935136A Effective fraction medicine for treating parkinson's disease The present invention relates to the application of apple polyphenol for preparing medicine and/or health-care product capable of curing and/or preventing Parkinson's disease. Its preparation process is simple and its therapeutic effect is good.
CN102205081A External liquid medicine capable of treating various skin diseases and preparation method thereof The invention discloses an external liquid medicine capable of treating various skin diseases, which comprises the following raw materials by weight: 20 to 30 grams of golden larch bark, 1 to 15 grams of cochinchina momordica seed, 10 to 15 grams of chinaroot greenbrier, 10 to 15 grams of common cnidium fruit, 10 to 15 grams of hydnocarpus seed, 10 to 15 grams of sessile stemona root, 8 to 12 grams of Chinese angelica, 4 to 6 grams of divaricate saposhnikovia root, 4 to 6 grams of evodia fruit, 8 to 12 grams of Chinese arborvitae twig, 10 to 15 grams of garden balsam flower, 10 to 15 grams ofpricklyash peel and 8 to 12 grams of lithargite. The external liquid medicine for treating the various skin diseases has the effects of killing insects, sterilizing, relieving itching, removing dampness, deodorizing, preventing cracks, relieving swelling and promoting tissue regeneration, has quick response and high cure rate, is safe and does not have toxic or side effects.
CA2355291C A pharmaceutical mixture comprising a profen A pharmaceutical mixture comprising a profen is described which has a profen content of over 85 % and contains up to 1% of a nonionic surfactant having an HLB of >=9 and also a customary disintegrant and a lubricant and optionally a microcrystalline cellulose.
WO2008129000A1 Pyridopyrimidine derivatives and use thereof in the treatment of itch and itch related disorders The invention provides the use of a compound of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the description, and combinations thereof, in the treatment of itch or an itch related disorder or disease.
CN102151547A Method for controlling adsorption, storage and release of guest molecules by using mesoporous material The invention discloses a method for controlling adsorption, storage and release of guest molecules by using a mesoporous material. The method comprises the following steps of: (1) preparing the mesoporous material, and reserving template agent micelles in synthetic raw powder of the mesoporous material; (2) after the mesoporous material prepared in the step (1) adsorbs the guest molecules at a high temperature, storing the mesoporous material at room temperature; and (3) raising the temperature in use so that the mesoporous material releases the guest molecules. Nano spaces are switched by regulating the flexibility of the micelles with temperature control to adsorb and release the guest molecules so as to realize storage and release under specific temperature control; a step of removing the template agent by roasting is reduced, environmental pollution is reduced, and the cost is lowered; the method can be used for complex systems of guest molecule carrying, medicament administration, microenvironment improvement and the like; and after the raw powder 353K synthesized by adopting MCM-48 mesoporous molecular sieves adsorbs NO, at most 38.13mu mol.g<-1> of NO can be released in acid solution simulating gastric fluid.
US20110195995 Methods of Optimizing Treatment of Estrogen-Receptor Positive Breast Cancers Estrogen-receptor positive and progesterone-receptor positive breast cancer treatment can be optimized by determining the level of expression of genes in a breast sample from a human having an estrogen-receptor positive and progesterone-receptor positive breast cancer that identify a human with an increased likelihood of recurrence of the breast cancer.
US20110166136 Calcium Ion Channel Modulators & Uses Thereof Compounds of formula (1), salts and pro-drugs wherein: R1, R2, R3 and R4 are hydrogen, alkyl, hydroxyalkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, nitro, amino, monalkylamino, dialkylamino, acylamino, alkoxycarbonylamino, alkylsulphonyl, arylsulphonyl, alkylsulphonylamino, arylsulphonylamino, aminosulphonyl or cyano, or any two of R1 to R4 that are adjacent on the ring may together represent the moiety —O—(CH2)n—O— wherein n is 1 to 3; R5 is hydrogen or alkyl; R6 is hydrogen or alkyl; and X is selected from the group consisting of: (a) groups of formula OR7 wherein R7 is hydrogen or alkyl which is optionally substituted with a substituent selected from alkylsulfonylalkyl, saturated or partially unsaturated heterocyclic, alkoxy, carboxyl, nitro, amino, monalkylamino, dialkylamino, halogen, and alkoxycarbonyl, provided that when R7 is hydrogen or ethyl, then R1, R2, R3 and R4 cannot be selected from hydrogen, halogen and alkyl; and (b) groups of formula NR8R9 wherein R8 and R9 together with the nitrogen atom to which they are attached form a saturated or partially unsaturated heterocyclic group which optionally contains at least one more heteroatom selected from nitrogen, oxygen and sulphur atoms, said saturated or partially unsaturated heterocyclic group optionally further being substituted by one or more substituents selected from alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, nitro, amino, monalkylamino, dialkylamino and hydroxyl, provided that: (i) when R8+R9+N=piperazine, and ≧1 of R1 to R4 are hydrogen, hydroxyl, nitro, amino, alkylamino, dialkylamino, alkoxycarbonylamino, halogen, alkoxy or alkyl, the nitrogen atom at the 4-position of the piperazine is not alkyl substituted, (ii) when each of R1, R2, R3, R4, R5 and R6 is hydrogen, X is not unsubstituted piperazinyl or unsubstituted morpholino, (iii) when each of R1, R2, R4, R5 and R6 is hydrogen and R3 hydrogen, bromine or hydroxyl, X is not methoxy, (iv) when each of R2 and R3 is methoxy or they together represent —O—CH2—O— and each of R1, R4, R5 and R6 is hydrogen, X is not unsubstituted piperidine, are Cavx channel blockers and are of use in the treatment of various conditions including pain.
CN103494789A Preparation method of sea-buckthorn polysaccharide soft capsule The invention discloses a preparation method of a sea-buckthorn polysaccharide soft capsule. The preparation method comprises the following steps: soaking sea-buckthorn pomace and hippophae rhamnosides in petroleum ether for 10-14 hours and then filtering; soaking the filtered sea-buckthorn pomace and hippophae rhamnosides for 10-12 hours by using new petroleum ether; after the petroleum ether naturally volatiles, adding distilled water and repeatedly boiling and extracting for 5 times till the solution is 1/10 of original volume, so as to obtain a sea-buckthorn polysaccharide material, wherein the ratio of sea-buckthorn pomace and hippophae rhamnosides to distilled water is 1:25 and each boiling and extracting lasts for 1 hour. According to the preparation method, the capsule can rapidly disintegrate inside a human body through optimal preparation of a capsule skin liquid, so that polysaccharide can be dissolved out favorably; rapid absorption of the polysaccharide inside a human body is facilitated by optimal preparation of contents, so that the functions can be taken. By adopting the soft capsule packing method, sea-buckthorn pomace, which is generated during production of a sea-buckthorn beverage factory is rich in polysaccharide and can be prepared into the soft capsules, so that the requirements of life preservation and health care of a consumer can be met, the primary products can be comprehensively used; waste materials are changed into precious materials; resources are saved.
WO2012028635A1 Deuterated analogs of pridopidine useful as dopaminergic stabilizers The present invention provides novel deuterated analogs of Pridopidine, i.e. 4-(3-methanesulfonyl-phenyl)-1 -propyl-piperidine. Pridopidine is a drug substance currently in clinical development for the treatment of Huntington's disease. In other aspects the invention relates to pharmaceutical compositions 10 comprising a deuterated analog of Pridopidine of the invention, and to therapeutic applications of these analogs.
US20080103159 Composition Comprising Ocaperidone The present invention relates to a composition comprising ocaperidone as an active substance and an effective amount of water-soluble polymers to increase solubility of ocaperidone. The present invention further relates to a therapeutic system for ocaperidone with a compartment for the drug formulation comprising said composition, and to a process for the preparation thereof as well as to the therapeutic use of said composition as antipsychotic drug. The present invention also relates to the solubilisation of ocaperidone in an aqueous medium with the aid of water soluble swellable polymers.
CN101862323A Application of 1,2-O-stearyl glyceraldehyde in preparing antibacterial agents The invention relates to the technical field of medicine, in particular to novel application of a compound 1,2-O-stearyl glyceraldehyde in preparing antibacterial agents. Proved by in vitro anti-bacteria tests, the 1,2-O-stearyl glyceraldehyde has obvious inhibiting effect on anthersmut, and the inhibiting effect of the 1,2-O-stearyl glyceraldehyde is even stronger than that of penicillin or streptomycin which is a positive control medicine, thus the 1,2-O-stearyl glyceraldehyde can be used for preparing the antibacterial agents. The invention provides a lead compound for developing novel antibacterial agents and has important significance for developing and utilizing Chinese ocean medicinal resources.
WO2010013011A1 P53 tumor suppressor protein activating The invention provides a compound of formula (I), wherein X, L1-4 and R1-4 are as defined herein, with the proviso that the compound is not (i) 4-benzoyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid ethyl ester; (ii) 4-(2,5-difluorobenzoyl)-3,5-dimethyl-1H-pyrrole-2-carboxylic acid ethyl ester); (iii) 4-acetyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid ethyl ester; or (iv) 4-(3-dimethylamino-acryloyl)-3,5-dimethyl-1H-pyrrole-2-carboxylic acid ethyl ester, or a pharmaceutically acceptable derivative thereof.
CN101829102A Application of methoxybenzene benzoyl silibinin in preparing medicine for treating viral hepatitis B The invention relates to an application of methoxybenzene benzoyl silibinin in preparing medicine for treating viral hepatitis B, in particular relates to an application of a silibinin esterified favonolignan compound substituted by 23-site 4-metoxybenzene benzoyl, or pharmaceutically acceptable salt thereof in preparing medicines for inhibiting HBV DNA replication, and treating hepatitis B virus infection diseases, wherein the favonolignan compound has exact inhibition activity to the hepatitis B virus, the inhibition activity thereof at 100 microgramme/mL to the HBV DNA replication of the hepatitis B virus is better than that of the alpha-interferon at the highest concentration of 10000 uint/mL, namely 47% higher than that of the inhibition activity of the alpha-interferon. The pharmacodynamics results show that the favonolignan compound or the pharmaceutically acceptable salt thereof can be expected to be used for preparing the medicine for inhibiting non-nucleoside HBV DNA replication or treating the hepatitis B virus infection diseases.
US20110039857 Piperidine and pyroolidine compounds The invention relates to piperidine and pyrrolidine compounds of formula (I) wherein A, B, n and X are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.
EP2056800A2 Therapy procedure for drug delivery for trigeminal pain The present invention relates to methods for the treatment or prevention of trigeminal nerve-associated pain, in particular chronic, acute and procedural-related pain. The methods comprise administration of analgesic agents to the trigeminal nerve system which results in analgesia to the facial or head region.
WO2013163404A1 TREATING VIRAL INFECTIONS HAVING VIRAL RNAs TRANSLATED BY A NON-IRES MEDIATED MECHANISM Provided herein are methods for preventing or treating a viral infection in a subject, wherein the viral infection is mediated by a virus comprising one or more viral RNA molecules translated by a ribosomal shunting mechanism or a non-IRES mediated mechanism. The methods comprise administering to a subject an agent that reduces ribosomal protein (Rps25) expression or function. Also provided are methods of inhibiting or promoting ribosomal shunting-mediated translation or non-IRES mediated translation. Also provided are methods of screening for an agent that inhibits or promotes ribosomal shunting-mediated translation or non-IRES mediated translation.
WO2008130619A3 A composition comprising an inhibitor of pde4 and/or pde7 Recombinant fission yeast cells and methods of using them are described, which provide for identification of chemical and biological inhibitors or activators of a target exogenous phosphodiesterase (PDE). The invention provides, in some aspects, compounds that inhibit cAMP PDE activity and compositions that include such compounds. The invention, in part, also includes methods of using cAMP PDE-inhibiting compounds in the treatment of cAMP PDE-associated diseases and/or disorders.
CN1957920B Anti cancer slow release agent carrying fluorouracil and synergist A slowly-release anticancer medicine in the form of injection or implant is disclosed. Said slowly-release injection is composed of a special solvent containing suspending aid and the slowly-release microballs consisting anticance medicine, iterstitial hydrolyte and slowly-releasing auxiliary. Said anticancer medicine is chosen from 5-FU, cisplatin, etc. Said interstitial hydrolyte is chosen fromcollagenase, relaxin, etc. Said slowly-releasing auxiliary is chosen from polylactic acid, FAD, polyethanediol, etc.
CN101378741A Method for treatment of neuropathic pain Compounds and methods useful for preventing and treating pain,e.g., neuropathic pain, in a subject in need thereof are provided. The compounds can be 'SlP modulating' agents that are capable of inducing a detectable change in SlP receptor activity.
WO2009139876A2 Regenerating and enhancing development of muscle tissue Muscle tissue regeneration is one of the most important homeostatic processes of adult skeletal muscle, which after development retains the capacity to regenerate in response to different type of stimuli, including a direct trauma or neurological dysfunction; atrophy; and genetic defects. The present invention pertains to cdk9-55 and its ability to regenerate muscle tissue and enhance development. Cdk9-55 is specifically induced upon satellite cell differentiation and is necessary for the gene expression reprogramming required to complete the regeneration process.
US20070292356 Biphenyl compounds useful as muscarinic receptor antagonists This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
EP1984331B1 Pyrrolidine derivatives as erk inhibitors Disclosed are the ERK inhibitors of Formula (1.0): and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (1.0).
US7534450 Promoting metallothioneins by administering a copper-free nutrient supplement containing 50 - 150 mg of zinc, and further containing vitamin B6, pyridoxal-5'-phosphate, vitamin E, vitamin A, vitamin C, selenium, glutathione, taurine, and a mixture of amino acids Provided by the present invention are novel and non-obvious nutrient supplements that preferably comprise minerals, vitamins, amino acids, and agents capable of delivering cysteine in vivo. The nutrient supplements desirably are capable of promoting metallothioneins, and optionally, promoting the removal of excess metals from the bloodstream. Also provided by the invention are methods of treating autism involving administration of the nutrient supplements. The methods include treatment to prevent or slow down the onset of autism once a predisposition for the development of autism has been detected, and treatment to alleviate or reverse the symptoms of autism once autism has been diagnosed. The invention further provides methods of administering the nutrient supplements in the treatment of other diseases, disorders and conditions, that would benefit from such administration, especially those that would benefit from metallothionein promotion and/or removal of excess metals from the bloodstream.
US20090099142 Pharmaceutical compositions comprising esterified estrogens and methyltestosterone and method of using same The present invention relates generally to pharmaceutical compositions comprising esterified estrogens, methyltestosterone and one or more pharmaceutical excipients. Methods for preparing and using such compositions are also provided.
CN102816090A Carbamate compounds, preparation method and application thereof The invention discloses novel carbamate compounds (I-1 to I-4) and pharmaceutically acceptable salts thereof, a preparation method of the compounds, and application of the compounds in preparation of medicines for preventing neurodegenerative diseases, including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV (human immunodeficiency virus) related cretinism, multiple sclerosis, progressive lateral spinal sclerosis, neuropathic pain, glaucoma and the like.
US7041680 (R) and (S) isomers of substituted 2-(2,6-dioxopiperidin-3-yl) phthalimides and 1-oxoisoindolines and methods of using the same Substituted 2-(2,6-dioxopiperidin-3-yl) phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl) isoindolines reduce the levels of TNFα in a mammal. Typical embodiments are 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafluoroisoindoline and 1,3-dioxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4-aminoisoindoline.
US7041305 Stable water in oil aminophylline emulsions A water in oil emulsion system and a process for preparing such a emulsion has been provided for topically applying aminophylline for reducing cellulite conditions.
CN102846723A Tuber fleeceflower root zinc lactate compound tablets and preparation method thereof The present invention provides tuber fleeceflower root zinc lactate compound tablets, which comprise the following components, by weight, 100-200 parts of tuber fleeceflower root micropowder, 1-2 parts of zinc lactate, 200-400 parts of a diluent, 7-20 parts of a binder, and 3-6 parts of a lubricant. The present invention further provides a preparation method for the tuber fleeceflower root zinc lactate compound tablets. The tuber fleeceflower root zinc lactate compound tablets prepared by the method of the present invention have double effects of the tuber fleeceflower root and the zinc lactate, and have characteristics of good anti-fatigue effect, good process performance, and simple and convenient preparation process.
CN101352505B Bone fracture setting medicine powder for treating traumatic injury The invention relates to a bone connecting powder for treating traumatic injury, which is made from 5 to 15 parts of daphne giraldii nitsch, 5 to 10 parts of saffron, 5 to 15 parts of notoginseng, 5 to 15 parts of chuanxiong rhizome, 5 to 10 parts of frankincense, 5 to 10 parts of myrrh, 6 to 20 parts of dragons blood, 5 to 15 parts of sappan wood, 10 to 20 parts of angelica, 5 to 15 parts of pyrite, 5 to 10 parts of ground beetle, 3 to 8 parts of hippocampus, 5 to 10 parts of rhizoma drynariae, 3 to 8 parts of pilose deer horn, and 1 to 3 parts of musk in definite weight proportion The fifteen bulk drugs are jointly ground into fine powder, and processed to particles with a fineness of 120 meshes, and then mixed evenly and made into pulvis. The powder of the invention has the functions of promoting blood circulation to dispel blood stasis, reducing swelling and alleviating pain, and promoting reunion of the fractured bones, and has apparent analgesic effect on soft tissue fracture, comminuted fracture and old injuries, the early-stage and medium-stage osteonecrosis, compression fracture of lumbar vertebra, bone lesion, lumbar disc protrusion and the like in the bone injury treatment. The powder of the invention has the advantages of quick effect-taking, good curative effect, short treatment course, convenient use, being safe and reliable, and no side effect. The clinical effective rate of the powder for more than 1200 cases is 96 percent.
US20070065868 IL-17 receptor like molecules and uses thereof Novel IL-17 receptor like polypeptides and nucleic acid molecules encoding the same. The invention also provides vectors, host cells, agonists and antagonists (including selective binding agents), and methods for producing IL-17 receptor like polypeptides. Also provided for are methods for the treatment, diagnosis, amelioration, or prevention of diseases with IL-17 receptor like polypeptides.
US20110190230 Betalain Compositions and Uses Thereof Contemplated compositions and methods employ betalains for treatment of various conditions, and especially osteoarthritis, sinusitis, contact dermatitis, acne, an allergic condition, reduced mental alertness, reduced physical strength, reduced physical endurance, and/or impaired mood.
US7309720 2-ethoxy-3-phenylpropionic acid derivatives for the treatment of lipid disorders A compound of formula (I) wherein T represents O, S or NR and wherein R represents a H, a C1-6alkyl group or a phenyl C1-6alkyl group and pharmaceutically acceptable salts thereof, processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and and pharmaceutical compositions containing them
CN102526741A Composition of arginine and series of cephalosporin acids The invention provides a composition of arginine and a series of cephalosporin acids. Due to the adoption of the composition, the characteristic of high antibacterial activity of cephalosporin acids is kept, and the problems of poor solubility and weak acidity of cephalosporin acids are solved; and the composition is suitable for being directly packaged into a powder injection for injecting. According to prediction, the composition has higher stability than a corresponding sodium salt preparation, and has a certain clinical practical meaning.
US20110136858 Preferred Combination Therapy Composition and use of a medicament comprising a fixed dose combination of droloxifene and clopidogrel, or the pharmaceutically acceptable salts thereof, for treating or preventing a disorder associated with the loss of normal adult tissue architecture.
WO2008043031A1 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II.
US20080249090 1-(4-(1H-pyrrol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one; modulators of kinase enzymes such as c-kit, and useful for the regulation of autoimmune disease(s), allergies, asthma, cancer and the like The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
US20050272647 Arthrodial cartilage extracellular matrix degradation inhibitor An agent for inhibiting articular cartilage extracellular matrix degradation of the present invention, comprising a histone deacetylase-inhibiting compound as an active ingredient, is effective for the prevention and treatment of diseases and pathological conditions involving the degradation and degeneration of the articular cartilage extracellular matrix, in particular, arthrosteitis, rheumatic arthritis, osteoarthritis, and the like.
WO2013157540A1 Nitrogen-containing heterocyclic compound or salt thereof The present invention addresses the problem of providing an Fms-like tyrosine kinase 3 (FLT3) inhibitor that is useful as a therapeutic agent for acute myeloid leukemia (AML). Provided is a novel nitrogen-containing heterocyclic compound represented by general formula [1] or a salt thereof. The compound according to the present invention or a salt thereof is usable as the active ingredient of a medicinal composition for treating diseases or conditions relating to FLT3 such as AML and acute promyelocytic leukemia (APL).
WO2011111880A1 Pharmaceutical composition for treating or preventing diseases caused by the nuclear export of gsk3, including a compound for inhibiting the nuclear export of gsk3 The present invention relates to a pharmaceutical composition for treating or preventing disease caused by the nuclear export of GSK3, including a compound for inhibiting the nuclear export of GSK3, and more specifically, to a pharmaceutical composition for inhibiting the growth or metastasis of cancer cells and including a novel compound for inhibiting the nuclear export of GSK3, and to a pharmaceutical composition for treating autoimmune diseases. According to the present invention, a composition for inhibiting the onset and progression of a disease caused by a decrease in GSK3 concentration in a cell nucleus through the nuclear export of GSK3 is provided. The compound according to the present invention is useful for treating or preventing various diseases by inhibiting the nuclear export function of GSK3 by Axin and increasing the concentration of GSK3 in the nucleus.
CN103263403A Application of borneol in preparation of drug used for inhibiting tumorigenesis The invention discloses application of borneol in preparation of a drug used for inhibiting tumorigenesis. In-depth research on application of borneol is carried out by using biomolecular means, and it is found that borneol exerts an inhibitory effect on a tumor through phosphorylation inhibition of a key protein on an NF-kB signal path of an inflammatory signal factor. Definite pharmacological effects enable application of borneol in inhibition of tumorigenesis to be more accurate; that is to say, borneol can substantially inhibit formation of a tumor in the stage of tumorigenesis, but borneol has no obvious inhibitory effect when the stage of tumorigenesis transits to the stage of proliferation of the tumor. Thus, borneol has remarkable application prospects in preparation of drugs used for inhibiting tumorigenesis, especially drugs for inhibiting formation of head and neck squamous cell carcinoma and activation of an NF-kB signal transduction system.
CN102000111A Preparation method of emergency survival hemostatic based on natural zeolite in Jinyun of Zhejiang The invention discloses a preparation method of an emergency survival hemostatic based on natural zeolite in Jinyun of Zhejiang. The emergency survival hemostatic takes natural clinoptilolite and natural mordenite in Jinyun of Zhejiang Province as raw materials and comprises main components of monox, titanium oxide, alumina, ferric oxide, magnesia, calcium oxide, sodium oxide, potassium oxide and the like. The emergency survival hemostatic can be used for different medical occasions to stanch bleeding, can be used for preparing band aids, transfusion plasters, self-adhesion dressing, first-aid packets and the like by being mechanically combined with other medical materials and medical instruments. Meanwhile, bacteriophage, anodyne and the like can be adsorbed in the emergency survival hemostatic by using the ion exchange characteristic of the emergency survival hemostatic; the emergency survival hemostatic can be used as a medical transmission carrier; and other ions can be loaded by using the ion exchange characteristic of the emergency survival hemostatic, thereby better curative effect can be obtained. The emergency survival hemostatic based on natural zeolite in Jinyun of Zhejiang has the advantages of high stanching speed, low heat release, asepsis, apyrogeneity, non-cytotoxicity, no sensitivity response, harmlessness to skin, no reducing substances, no acid-base excitability and low cost, can extract content heavy metal with extremely-low content and is convenient for use.
CN1682734A Oral disintegration tablet of dihydroergotoxine and its derivatives and its preparing process The present invention provides a kind of oral disintegrating tablet with the functions of exciting dopamine and 5-hydroxytryptamine acceptor, blocking alpha-adrenoceptor effect and dilating blood vessel, and the oral disintegrating tablet contains dihydroergotoxine or its derivatives as the active medicine component. By using dihydroergotoxine or its derivatives as main material and adding stuffing, disintegrating agent, corrective, flow assistant, lubricant and other supplementary material, the oral disintegrating tablet is prepared through specific process. The oral disintegrating tablet has excellent crisp disintegrating performance, fast disintegration, good taste and other features. Especially, it can improve patient's compliance to raise the curative effect of medicine.
US20090075861 Systems and methods of removing and managing heavy metals Systems and methods remove and manage heavy metals. In one implementation, an exemplary method can be applied to food processing and food consumption to remove heavy metals such as mercury, lead, uranium and cadmium before absorption by a living organism. The exemplary method exposes the food to a heavy-metal binding ligand, such as a concentrated protein or phytic acid, to form a heavy-metal chelate, and then allows the chelate to separate from the food. In another implementation, an exemplary probe possesses innovative molecular layers on its surface to detect and quantify heavy metals by attracting and binding traces of the heavy metals on a ligand layer.
US20110172241 Benzazole analogues and uses thereof The present invention relates to compounds of the general formulas (I), (Ia) and (II) and salts and physiologically functional derivatives thereof, wherein the substituents —Y are attached to the 5- or 6-position of the benzazole.
WO2012077127A1 A protein free surfactant composition for pulmonary diseases and a process for preparing the same A protein free surfactant composition comprising dipalmitoylphosphatidyl choline (DPPC) and eugenol having a ratio in the range of 10:5 to 4:2 with >99% airway patency in the presence of albumin, for treating acid lung injury, adult respiratory distress syndrome and meconium aspiration syndrome.
CN101987201A Medical ultrasonic probe sterilizing gel and preparation method thereof The invention provides a medical ultrasonic probe stelrizing gel and a preparation method thereof. The gel comprises the following components of 0.5-5 percent (w/v) of non-ionic cellulose material or 5-20 percent (w/v) of poloxamer, 0.1-0.5 percent (w/v) of chlorhexidine acetate, 0.1-0.5 percent (w/v) of double-chain quaternary ammonium salt sterilizing agent, 0.5-2 percent (v/v) of wetting agent and the balance of water. The sterilizing agent has the function of sterilizing and disinfecting a medical ultrasonic probe and the skin; and a soluble medical ultrasonic probe sterilizing gel with better acoustical property, safety and stability can be used as a coupling agent, can realize high-efficiency sterilization within short time and concurrent disinfection on the ultrasonic probe, and achieves the purpose of reducing cross infection risk caused possibly in the clinical ultrasonic detection process.
WO2009158309A3 Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists The present invention provides novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists useful in the treatment of conditions such as hypertension and other diseases.
CN102755390A Cough relieving and phlegm eliminating electuary lozenge and preparation method thereof The invention relates to a cough relieving and phlegm eliminating electuary lozenge and a preparation method thereof. The preparation method is a texture preparation method. The electuary lozenge comprises the following components in percentage by weight: 0.01-0.20 percent of liquorice infiltration cream, 0.0002-0.003 percent of opium powder, 0.0001-0.003 percent of star aniseed oil, 0.0001-0.003 percent of camphor, 10-80% of white honey, 5-95 percent of sugar and 0.01-10% of auxiliary material. The preparation method of the cough relieving and phlegm eliminating electuary lozenge comprises the steps as follows: (1), the liquorice infiltration cream, the opium powder, the star aniseed oil, the camphor and the white honey are taken according to a proportion, mixed together and stewed to be a thin liquid; (2), the sugar and the auxiliary material are mixed together according to a proportion and stewed to be a thin liquid; and (3), the medicine which is stewed to be a thin liquid and the sugar and the auxiliary material which are also stewed to be a thin liquid are placed according to a proportion into a die at the same time, so that the electuary lozenge which is well-bedded and is clear in texture is obtained, and is cooled and formed.
CN101157668B Substituted cinnamic acid nitrogen-containing derivative having tumor cytotoxic activity The invention relates to a substituted cinnamic acid nitrogen-containing derivative which has a structure of formula (I) and cytotoxic activity and the medical salts and solvates, and the invention further relates to a preparation method of the compounds with the formula (I), a pharmaceutical composition and a medical usage. The compound of the invention has stronger activity to inhibit the growth of the tumor cells of human esophageal cancer (Eca-109) and poorly differentiated gastric adenocarcinoma (BGC 823), which can be expected to be used as an antitumor drug.
CN101721395A Water soluble gel containing xylitol and application thereof in medicine for treating cervical erosion The invention relates to water soluble gel containing xylitol and carrying out internal administration through the local vagina and an application thereof in preventing and treating a uterine cervix disease named as cervical erosion.
US20120115844 Novel triazole compounds i The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A α5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
US8211891 Difluoromethyl-containing macrocyclic compounds as hepatitis C virus inhibitors The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
US20070043084 1,2-Diarylimidazoles useful as inhibitors of cox A compound of the formula (1): wherein R1 is cyano, and the like; R2 is hydroxy, and the like; R3 is (lower)alkoxy, and the like; X and Y are each CH or N; or pharmaceutically acceptable salts thereof, which are useful as a medicament.
US7507563 culturing propionibacterium under anaerobic conditions, in medium containing a carbon source such as lactose, to form 1,4-dihydroxynaphthalene-2-carboxylic acid, having a good flavor, useful for foods, beverages and drugs A process for producing 1,4-dihydroxy-2-naphtoic acid, comprising initiating the culture of 1,4-dihydroxy-2-naphthoic acid producing bacteria belonging to propionic acid bacteria under anaerobic conditions and culturing the bacteria under aeration into a medium when the concentration of a carbon source in the medium is 3.5% by mass or less.
CN102727434A Veterinary enrofloxacin nanoemulsion The present invention relates to a veterinary enrofloxacin nanoemulsion, which comprises the following raw materials, by weight, 2-10 parts of enrofloxacin, 5-15 parts of trichloromethane, 20-40 parts of propylene glycol, 10-20 parts of linseed oil, 5-10 parts of polyethylene glycol 400, 10-20 parts of Tween 80, and 15-30 parts of water. With the nanoemulsion of the present invention, solubility of the enrofloxacin in the water is improved, drug dispersion degree is increased, and contact chance of the drug and the outer phase is reduced so as to improve bioavailability and stability of the drug.
US7291622 Administering a 4-Amino-2-[1-(o-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinylcarbamate derivative, optionally mixed with an organic nitrate or NO donor or a cGMP inhibitor for treating sexual dysfunction This invention relates to methods for treating sexual dysfunction, by administering a compound of the formula wherein R1 is H or a di-C1-6-alkylaminocarbonyl radical, and R2 is a radical of the formula —O—C(X)—NR3R4 wherein X is O or S. The compound may also be administered in combination with at least one organic nitrate or NO donor, or in combination with at least one compound which inhibits the breakdown of cyclic guanosine monophosphate (cGMP).
EP1692097B1 Tricyclic hydroxamate and benzamide derivatives, compositions and methods The present invention relates to compounds and methods for inhibiting histone deacetylase enzymatic activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit histone deacetylases (HDACs), and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, and also central nervous system diseases. It further deals with processes for preparing said compounds.
US7868005 Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
US8728488 Methods of inducing an immune response in a host by administering flavivirus immunogens comprising extracellular viral particles composed of the premembrane (prM) and envelope (E) antigens The invention encompasses nucleic acid molecules containing transcription units which encode the flavivirus M and E protein antigens. The flaviviruses include Japanese encephalitis virus, dengue, yellow fever virus and St. Louis encephalitis virus. The nucleic acids function to provide the M and E protein antigens when the nucleic acid resides in an appropriate host cell, especially when the host cell is the cell of a subject. The invention also encompasses a vaccine whose active agent is the nucleic acid. The invention further encompasses the cultured host cells when they contain within them nucleic acid molecules containing the transcription units. The invention in addition encompasses a method of immunizing a subject against flavivirus infection by administering to the subject an effective amount of a vaccine containing a nucleic acid molecule containing the transcription unit of the invention.
WO2009147440A1 Heterocyclic urea derivatives and methods of use thereof Chemical Compounds Compounds of formula (I)and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
CN101279089B Donkey-hide gelatin calcium composition and preparing process thereof The invention relates to a combination of donkey-hid gelatin and calcium and a preparation method thereof, which pertains to the preparation field of medical nutrition. Iron-deficiency and calcium deficiency exist at the same time, when a person supplements the calcium in a large dosage, the calcium inhibits the body to absorb the iron elements and impacts the effect of blood enriching; in order to overcome the problem, the invention discloses a formula of the combination of donkey-hid gelatin and calcium; the formula not only comprises donkey-hid gelatin, calcium lactate, calcium gluconate, but also the iron-supplementing agent of ferrous fumarate, the calcium and iron absorption enhancer of casein phosphopeptide and excipients acceptable by pharmacology. The combination realizes the purpose of supplementing the calcium and the iron at the same time, thus having the advantages of reducing types of medicines taken by a patient, improving nutritional anemia, enhancing bone mineral density and reducing economic burden of the patient.
CN101029065B Bean-curd pectin analogue and its use in medicine for preventing depression An application of helicidum analog in preparing medicines for preventing and treating depression is disclosed. Its chemical structure is also disclosed.
CN102579317A Cantharidin vesicles and preparation thereof and preparation methods of cantharidin vesicles and preparation thereof The invention discloses cantharidin vesicles and a preparation method thereof, and a preparation containing the cantharidin vesicles and a preparation method thereof, and belongs to the field of pharmaceutical preparations. The cantharidin vesicles are prepared from cantharidin, a nonionic surfactant and an additive and are preferably prepared into an external gel preparation. A cantharidin percutaneous delivery external preparation has unique advantage over the medicament and is applied to a novel vesicle administration system, so that the percutaneous absorption of the medicament is increased, the clinical curative effect is enhanced, and the cantharidin percutaneous delivery external preparation can be used for treating cancer, specifically liver cancer, and has a liver targeting effect.
US20080181937 Vitamin C, Vitamin E, DHA and Curcumin; treating an individual who is at increased risk of developing Alzheimer's disease because of family history Methods and compositions for preventing memory loss and reducing the onset of Alzheimer's disease and the pathological symptoms associated therewith including memory loss, reduced cognitive function and dementia are provided. These methods and compositions comprise dosage regimens that provide for the daily administration of effective amounts of Vitamin C, Vitamin E, DHA, and Curcumin.
CN1895278A Medicine for treating gastropathy and duodenal ulcer A medicine in the form of capsule for treating gastric ulcer and duodenal ulcer is prepared through baking and grinding chicken's gizzard-skin, proportionally mixing it with oxytetracycline and furazolidone, and filling the mixture in capsules.
CN103505657A Belly patch for treating intestinal dysfunction after abdominal cavity surgery and preparation method of belly patch The invention discloses a belly patch for treating intestinal dysfunction after abdominal cavity surgery and a preparation method of the belly patch, and solves the problem of the intestinal dysfunction after the abdominal cavity surgery. The invention is characterized in that the preparation method comprises the following steps: (1) distilling tall gastrodia fruit, alyxia sinensis and pimpinella diversifolia with steam, and collecting volatile oil and residues for standby use; (2) grinding azurite and charred rice sprouts into fine powders for standby use; (3) thoroughly mixing aspongopus, timonius arboreus, jasminum grandiflorum flower, allium victorialis, spatholobus stem, flueggea suffruticosa, ramulus cinnamomi and residues obtained from the step (1), extracting with ethanol twice, mixing the extraction liquids, filtering, recovering ethanol and concentrating under reduced pressure to obtain a soft extract; (4) adding the fine powders from the step (2) into the soft extract from the step (3), oven-drying at 60 DEG C, grinding into fine powder, adding polysorbate-80, making granules, oven-drying, grading, spraying with the volatile oil obtained from the step (1), thoroughly mixing, packaging and applying to the bellybutton. Clinical trials show that the belly patch has the characteristics of good curative effect and relatively high safety, and is worthy of clinical application and promotion.
CA2781194A1 Reducing inflammation using cell therapy The invention provides methods for treating pathological conditions associated with an undesirable inflammatory component, including graft- versus -host disease. The invention is generally directed to reducing inflammation by administering cells that express and/or secrete prostaglandin E2 (PGE2). The invention is also directed to drug discovery methods to screen for agents that modulate the ability of the cells to express and/or secrete PGE2, such as PGE2 receptor agonists. The invention is also directed to cell banks that can be used to provide cells for administration to a subject, the banks comprising cells having desired levels of PGE2 expression and/or secretion. The invention is also generally directed to delivering cells directly to lymphohematopoietic tissue, such as spleen, lymph nodes, and bone marrow. The invention is, thus, also directed to a method for treating inflammation by administering cells directly into sites of lymphohematopoiesis, such as spleen, lymph nodes, and bone marrow. The administered cells include those that reduce the activation and/or proliferation of T-cells. Such cells may or may not express and/or secrete PGE2.
CN103550788A Health-care method for improving immune effect of livestock and poultry vaccine and reducing immunological stress The invention provides a health-care method for improving an immune effect of a livestock and poultry vaccine and reducing immunological stress and provides an immunity-enhancing health-care method applied aiming at the process of carrying out vaccination on livestock and poultries. The health-care method specifically comprises the following steps: in each time of vaccinating, a specific medicine taking method comprises the following steps: a first medicine is taken at the day before immunization; a second medicine is taken at the day of the immunization; a second medicine is taken three days after the immunization. According to the health-care method, the immunity and the distance resisting capability of organisms of the livestock and poultries can be improved obviously; the vaccine immune effect is enhanced; the immunity is successful; the vaccine stress reaction is reduced.
US20090124611 Pyrazolopyridine-1,4-Diamines and Analogs Thereof Pyrazolopyridine-1,4-diamines and analogs thereof, e.g., pyrazolo[3,4-c]pyridine-1,4-diamines, pyrazolo[3,4-c]quinoline-1,4-diamines, 6,7,8,9-tetrahydro pyrazolo[3,4-c]quinoline-1,4-diamines, and pyrazolo[3,4-c]naphthyridine-1,4-di-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
CN101928245A 8-hydroxyl or methoxyl-2-aryl-1-isoquinolines, synthesis method and application thereof The invention discloses 8-hydroxyl or methoxyl-2-aryl-1-isoquinolines, a synthesis method and application thereof. Chemical structural formula of the 8-hydroxyl or methoxyl-2-aryl-1-isoquinolines is shown in I, wherein X expresses hydroxyl or methoxyl; Ar expresses aryl; and R expresses 5-methoxyl, 6-methoxyl or 6-methoxyl-5-amido. The 8-hydroxyl or methoxyl-2-aryl-1-isoquinolines are 8-hydroxyl or methoxyl-2-aryl-1-isoquinoline derivatives or pharmaceutically acceptable salts thereof. The 8-hydroxyl or methoxyl-2-aryl-1-isoquinolines have novel structure and easy implementation of synthesis method. Antitumor activity tests show that the 8-hydroxyl or methoxyl-2-aryl-1-isoquinolines have remarkable growth inhibition effect on human lung gland cancer cells A549 and human skin cancer cells A431; and most of the 8-hydroxyl or methoxyl-2-aryl-1-isoquinolines have stronger activity compared with Gefitinib.
WO2013143300A1 Sustained-release preparation of fulvestrant or derivatives thereof and preparation method therefor Disclosed are a sustained-release preparation of fulvestrant or derivatives thereof and a preparation method therefor. The formulation of the preparation is as follows: (1) fulvestrant or derivatives thereof, with a content of 10mg/ml-500mg/ml in the preparation, (2) ketone compound or dimethyl sulfoxide as the cosolvent, possessing a content of 3%-80% in the total weight of the preparation, (3) vegetable oil or artificially synthesized oil (ester) as the dispersing agent, (4) analgesic, and (5) an optional antioxidant.
CN101987102A Ophthalmic anti-inflammatory composition of glucocorticoid heteroaryl sulfamoyl carboxylate The invention relates to an ophthalmic anti-inflammatory composition of glucocorticoid heteroaryl sulfamoyl carboxylate, which comprises a sulfamoyl carboxylate compound represented by the formula (II) as an active component and one or more than one pharmaceutic adjuvant pharmaceutically and directly acting on the eyes, wherein X is unsubstituted or substituted heteroaryl or alkyl heteroaryl, Drug is a steride compound which can form carboxylate through OH groups, and X and Drug can be optionally substituted.
CN1765937A Bismuth potassium hyalurate and its preparation method and uses The hyaluronic-acid bismuth salt has chemical formula as (C14O13NH21Bi)m(C14O11NH19K)n, wherein, m:nú¢1:0.01~20, to which, the preparation method comprises: taking reaction between soluble hyaluronic-acid salt and bismuth salt in caustic potash liquid, depositing, cleaning, filtering, and drying. This product can be used in the drug for gastrointestinalulcer with better curative effect to similar products shown by animal testing.
CN1666736A Compound Tramadol Hydrochoride dispersible Tablet The invention relates to one agent type of compound tramadol hydrochloride. The provided technical project produces tramadol hydrochloride and acetyltropolone dispersible tablet with following components in weight fractions: tramadol hydrochloride in 37.5 deals; acetyltropolone in 325 deals; filling agent in 15-25 deals selected from lactose, compressible starch, white dextrine and/or starch; disintegrating adminicle in 50-70 deals selected from crosslinked polyvinyl pyrrolidone, microcrystalline cellulose, L-HPC, sodium carboxymethylstarch and/or compressible starch; lubricating agent in 1-2.5 deals selected from magnesium or/and talcum powder. The time of dispersing uniformly of provided dispersible tablet can reach 1 minutes and the time limit of disintegrating can reach 2 minutes.
US20090069426 Methods For Reducing The Amount Of A Proinflammatory Substance In Animal Tissue Or Body Fluid A method for reducing the amount of a proinflammatory substance present at an elevated level in animal tissue or body fluid by orally administering to the animal a proinflammatory substance reducing amount of a composition comprising at least one omega-3 fatty acid. The method is useful for reducing inflammation caused by elevated levels of proinflammatory substances including inflammation associated with an oral condition.
US20120027752 Methods and compounds for treating paramyxoviridae virus infections Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein the 1′ position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Human parainfluenza and Human respiratory syncytial virus infections.
WO2014040938A1 Non-annulated thiophenylamides as inhibitors of fatty acid binding proteini(fabp) 4 and/or 5 The invention provides novel compounds having the general formula (I), wherein R1, R2, R3, R4, R5, R6 , R7, A, E and n are as described herein, compositions including the compounds and methods of using the compounds.
WO2011138665A1 Novel immunomodulator and anti inflammatory compounds The present invention provides dihydroorotate dehydrogenase inhibitors of formula (I), methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.
US20050267032 Sulfone-containing prodrugs Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides sulfone-containing prodrugs, and compositions and methods utilizing sulfone-containing prodrugs that are useful in the treatment of diseases by blocking potassium channels associated with the onset or recurrence of the indicated conditions. Exemplary diseases treatable with the compounds, compositions and methods of the invention include sickle cell disease and glaucoma.
CN102688202A Temozolomide freeze-dried preparation The invention relates to a temozolomide freeze-dried preparation, which contains a temozolomide active ingredient and at least one solubilizer which can dissolve the temozolomide. The solubilizer used in the preparation may be N(2)-L-Alanyl-L-glutamine, glycyl-L-glutamine monohydrate, glycyl-l-tyrosine, ornithine aspartate or a mixture of the four. The temozolomide preparation prepared by using the technology provided by the invention has the advantages that the solubility of the temozolomide and the stability of the solution are improved; the quality of the solution is stable; the use of thepreparation is convenient; and the preparation method is simple and suitable for large-scale preparation.
US20110110859 Protein The present invention provides methods and compositions for screening, diagnosis and prognosis of colorectal cancer, for monitoring the effectiveness of colorectal cancer treatment, and for drug development.
EP1882687A1 Heterocyclic compounds useful as vanilloid receptor antagonists and pharmaceutical compositions containing the same This present invention relates to novel compounds, of the formula (I), isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1;VR1;TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, inflammatory disease of the joints, neuropathies, HIV-related neuropathy, nerve injury, neurodegeneration, stroke, urinary bladder hypersensitivity including urinary incontinence, cystitis, stomach duodenal ulcer, irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD), fecal urgency, gastro-esophageal reflux disease (GERD), Crohn's disease, asthma, chronic obstructive pulmonary disease, cough, neurotic/allergic/inflammatory skin disease, psoriasis, pruritus, prurigo, irritation of skin, eye or mucous membrane, hyperacusis, tinnitus, vestibular hypersensitivity, episodic vertigo, cardiac diseases such as myocardial ischemia, hair growth-related disorders such as effluvium, alopecia, rhinitis and pancreatitis.
CN103494877A Composition for treating scar and preparation method thereof The invention discloses a composition for treating a scar and a preparation method thereof. The composition for treating the scar comprises carboxylic polyether polysiloxane, polycarbophil, lavender essential oil, asiaticoside, a transdermal enhancer, allantoin, glycerol, triethanolamine and triclosan. The drug can directly reach impaired skin tissues effectively, enhance the cell viability, soften scars, relieve scar formation, repair broken fibers, repair a collagen structure of a skin base layer, and discharge and assimilate pigments of scar tissues; meanwhile, cell regeneration is effectively facilitated and the pigment of the damaged skin is balanced, so that the skin restores normal skin color.
CN102382128A Three-ring fused PI3K and mTOR dual inhibitor The invention belongs to the technical field of medicine and specifically relates to a three-ring fused PI3K and mTOR dual inhibitor, its pharmaceutically acceptable salt or stereoisomer shown by the general formula (I), in which R1, R2, R3, R4 and X are defined as in the instruction. The invention also relates to preparation methods of the compounds, pharmaceutical preparations containing the compounds, combinations containing the compounds and applications of the compounds in the preparation of drugs for treating and/or preventing proliferative diseases.
WO2011013909A3 Composition containing oligo-hyaluronic acid for promoting the stemness of skin cells and for stimulating differentiation The present invention relates to a composition containing oligo-hyaluronic acid for promoting the stemness of skin cells and for stimulating differentiation, and more specifically, to a composition containing oligo-hyaluronic acid as an active ingredient for promoting the stemness of skin cells and for stimulating differentiation, and to a method for stimulating the differentiation of adult skin stem cells using same. According to the present invention, unlike existing hyaluronic acid, oligo-hyaluronic acid exhibits the effects of stimulating differentiation in epidermal cells and enhancing the function of epidermal cells by increasing the expression of markers of the epidermal stem cells in skin tissue to restore the stemness of the epidermal cells.
EP1742922A1 Crystalline pyrazole derivative The present invention relates to crystal forms of 4-[5-(4-fluorophenyl)-3(trifluoromethyl)-1H-pyrazol-l-yl]-benzenesulfonamide and methods for preparation, interconversion, and isolation of such crystals.
WO2013130603A1 Ganglioside gd2 as a marker and target on cancer stem cells Methods for determining the presence of cancer stem cells by detecting GD2 expression. Also provided are methods for reducing proliferation of cancer stem cells by contacting the cells with a GD2 targeting agent, such as an anti-GD2 antibody or a GD3 synthase inhibitor. GD3 synthase inhibitor compounds are also provided.
US20100016295 Preparation and Use of Biphenyl Amino Acid Derivatives for the Treatment of Obesity This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
CN101037689A Anti-sense nucleotide of c-erbB2 cancer gene combined with epidermal growth factor and its application The invention provides a antisense short nucleotide of c-erbB2 cancer gene whose sequence is: SEQ ID NO 1. The antisense short nucleotide is combined with epidermal growth factor by Poly-L-Lysine, injecting the vinculum into tumour cell of body, EGFR receptor and c-erbB2 both belong to epidermal growth factor receptor family with distributed conformity and consanguinity in organisation, so increasing ratio of target/nontarget, raising diagnostic sensibility and treatment effect of antisense gene for excess expressed cancer of c-erbB2 cancer gene.
US20070082957 2-chloro-5-(3-oxopropyl)-N-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-benzamide; P2X7 receptor antagonists; inflammatory, immune or cardiovascular diseases The invention provides adamantane derivatives of formula (I), a process for the their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).
US7101911 Bis(substituted propynyl)-substituted benzenes, pyridines, pyrimidines, pyrazines, pyridines, furans and pyrroles; e.g., 3,5-bis-(3-(4-aminomethylbenzylaminocarbonyloxy)prop-1-ynyl)--1 -hydroxymethylbenzene Compounds of the formula I, in which M, A1, A2, K1 and K2 have the meanings given in the description are novel effective tryptase inhibitors.
WO2011016749A1 Combined anti-tuberculosis composition The invention relates to medicine and concerns a combined medicinal preparation which has anti-tuberculosis activity and is in a solid dosage form which contains, as the active principle, a combination of p-aminosalicylic acid and a zinc-containing compound and pharmaceutically acceptable auxiliary substances. The claimed composition is characterized by being highly effective.
US8685994 Analgesic combination of oxycodone and celecoxib Disclosed is a pharmaceutical composition, comprising two analgesic compounds and/or pharmaceutically acceptable salts thereof consisting of celecoxib and/or at least one pharmaceutically acceptable salt thereof and oxycodone and/or at least one pharmaceutically acceptable salt thereof, said two analgesic compounds in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising orally administering to the patient an oral dosage form comprising two analgesic compounds consisting of celecoxib and/or at least one pharmaceutically acceptable salt thereof and oxycodone and/or at least one pharmaceutically acceptable salt thereof, said two analgesic compounds in an amount sufficient to provide an analgesic effect in a human patient.
US20080044361 The invention relates to propellant gas formulations containing suspensions of the crystalline monohydrate of (1 7-((hydroxydi-2-thienylacetyl)oxy)-9, 9-dimethyl-3-oxa-9-azoniatricyclo(3.3.1.02,4)nonane-bromide, with a simple monoclinic cell, and one or more adjuvants The invention relates to propellant gas formulations containing suspensions of the crystalline monohydrate of (1α,2β,4β,5α,7β)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane-bromide.
DE102010008642A1 New 5'-biphenyl substituted cyclic ketoenol compounds are acetyl-coenzyme A carboxylase 1 inhibitors, useful for treating cancer e.g. breast cancer, pancreatic cancer, renal cell carcinoma, hepatocellular carcinoma and skin tumors 5'-Biphenyl substituted cyclic ketoenol compounds (I), are new. 5'-Biphenyl substituted cyclic ketoenol compounds of formula (I), are new. X : 1-3C alkyl or 1-3C alkoxy (both optionally substituted by at least a halo) or halo; W1, Y1 : H, halo or 1-3C alkyl (optionally substituted by at least a halo); either V1-V3 : H, halo, 1-3C (halo)alkyl, 1-3C (halo)alkoxy or 1-3 alkoxy-1-3C; or C+V1+V2 : optionally saturated and optionally at least a further heteroatom containing 5 or 6 membered cycle T1 (optionally substituted by one or more halo and/or 1-3C alkyl); either A : 1-6C alkyl- or 1-6C alkoxy-1-6C alkyl (both optionally substituted by at least a halo), 3-7C cycloalkyl or 4- to 7-membered monocyclic heterocyclyl (both optionally substituted by one or more halo and/or 1-3C alkyl) or H; and B1 : H, 1-6C alkyl or 1-3C alkoxy-1-3C alkyl; and D1 : 1-6C alkyl, 1-6C alkoxy-1-6C alkyl, 3-7C cycloalkyl or 4- to 7-membered monocyclic heterocyclyl (all optionally substituted by one or more halo, OH, 1-3C alkyl, halo-1-3C alkyl, 1-3C alkoxy, halo-1-3C alkoxy and/or 1-3C alkoxy-1-3C alkyl) or H; or C+A+B1 : optionally saturated, optionally one or two heteroatoms containing 3-8 membered cycle T2 (optionally substituted by one or more R1-R3); or A+D1 : optionally saturated and optionally a further heteroatom-containing 5-7 membered cycle T4 (optionally substituted by one or more R7-R9); R7-R9 : halo, 1-3C alkyl or 1-3C alkoxy; either R1-R3 : 1-4C alkyl, 1-4C alkoxy, 1-3C alkoxy-1-3C alkyl, 1-3C alkoxy-1-3C alkoxy, halo-1-3C-alkyl or halo-1-3C alkoxy (all optionally substituted by OH in alkyl residue), halo or OH; or two of R1-R3 together with cycle T2 : saturated or aromatic, optionally one or two heteroatoms containing 5-7 membered cycle T3 (optionally substituted by one or more R4-R6); and R4-R6 : 1-3C alkyl or 1-3C alkoxy. [Image] - ACTIVITY : Cytostatic; Antipsoriatic; Vulnerary. - MECHANISM OF ACTION : Acetyl-coenzyme A carboxylase 1 inhibitor; Acetyl-coenzyme A carboxylase 2 inhibitor. The ability of (I) to inhibit acetyl-coenzyme A carboxylase 2 was tested in vitro. The results showed that 3-(4'-chloro-4,6-dimethylbiphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspir o[4.5]dec-3-en-2-one exhibited an IC 5 0value of 0.087 mu ole/l.
CN102641277A Ointment for treating gynaopathy and dermatoses and preparation method thereof The invention discloses an ointment for treating gynaopathy and dermatoses and a preparation method thereof. The externally-applied ointment is prepared from halcinonide preparation, menthol crystal and camphor which are utilized as raw materials according to a certain preparation technology, and is prepared from the following raw materials in parts by weight: 6 to 6.5 parts of halcinonide preparation, 15 to 20 parts of menthol crystal, 15 to 20 parts of camphor, 3 to 3.5 parts of edetate disodium, 20 to 40 parts of polyethylene glycol mono stearate, 0 to 3 parts of essence, 0 to 2 parts of carbomer, 0 to 2 parts of sodium bicarbonate and 15 to 25 parts of pure water. The externally-applied ointment is low in cost, has the effects of clearing away heat, eliminating dampness, dispelling the wind, killing worms, diminishing inflammation and relieving itching, has better treatment effects, has the characteristics of being easy to prepare, lower in cost and obvious in treatment effect, and can be used for treating the gynaopathy, such as vaginitis, cervicitis and cervical erosion, caused by various germs, and treating the dermatoses, such as tinea corporis, tinea cruris, tinea of feetand hands and various dermatitis, caused by various fungus infection. The externally-applied ointment has exact treatment effects, takes effect rapidly, is low in cost and convenient to use, and has no toxic and side effects, thus being worthy of popularization and application.
US20050152989 Method for treating irritable bowel syndrome The invention provides a method for treating irritable bowel syndrome, comprising administering an osmotic laxative and fiber in a therapeutically effective regimen to a patient in need of such treatment. The therapeutically effective regimen includes administering the formulation in a dose and at a frequency and duration sufficient to reduce or eliminate the symptoms of irritable bowel syndrome or to provide symptomatic or palliative relief to the patient.
CN1887260A Slow released compound anticancer injection containing clorfarabine The slow released compound anticancer injection containing clorfarabine consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is the composition of clorfarabine with alkylating agent, purine analog and/or hormone anticarcinogen. The slow releasing supplementary material is polylactic acid and its copolymer, polyethylene glycol, EVAc, etc or their composition. The .suspending agent is carboxymethyl cellulose, etc. and has viscosity of 80-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent. The present invention can inhibit the growth of tumor and enhance the curative effect of chemotherapy, radiotherapy and other non-operative treatment.
US20110288135 Fast Dissolving Tablet The present invention relates to processes for the preparation of tablets which dissolve rapidly in the mouth and provide an excellent mouthfeel. The tablets of the invention comprise a compound which melts at about 37° C. or lower, have a low hardness, high stability and generally comprise few insoluble disintegrants which may cause a gritty or chalky sensation in the mouth. Convenient and economically feasible processes by which the tablets of the invention may be produced are also provided.
US20080214629 Administering a dosage form of 6-20 mg of tizanidine; plasma drug concentration substantially ascends over a period of 8 hours following administration The present invention relates to a novel controlled release formulations of tizanidine. The invention also provides methods of using novel controlled release formulations of tizanidine to treat a patient.
US20080039441 Storage stability; combination forms with antidepressants, antiinflammatories, serotonin reuptake inhibitors, antiemetics, appetite modulators, antivirals, vasodilators and/or pain relievers The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.
EP1351673B1 Compositions of stable t3 and use thereof This invention provides a stable composition containing T3 serum albumin and water, wherein the T3 has a half-life of at least five days, particularly at neutral pH. This ivention further provides a method for emergency treatment of a patient with cardiac arrest and with cardiac electrical standstill to restore effective cardiac function, comprising administering to the patient a therapeutically effective amount of stable composition.
US20090318379 Statins for the Treatment of Viral Influenza Infections The present invention relates to methods for the treatment of viral influenza using statins, or pharmaceutically effective salts, pro-drugs or metabolites thereof. In particular it is disclosed that statin hydroxyl acid salts including, but not limited to, mevastatin, lovastatin, pravastatin and simvastatin, are effective in conferring resistance to infection with influenza type A viral challenge.
US20120316240 Method of diagnosis Disclosed herein are methods that generally to the fields of pharmaceutical chemistry, biochemistry, molecular biology and medicine. More particularly, aspects of the invention concern methods to identify a predisposition for fibrosis in a biological sample, methods of identifying agents that modulate the onset of fibrosis, methods of making a formulation that inhibits the onset or progression of fibrosis, and methods of monitoring the progression of fibrosis or the efficacy of a fibrosis treatment.
US20090175928 Lip Plaster The invention relates to a self-adhesive lip plaster which comprises at least one single-layered matrix and which contains at least one antiviral active medical substance for using in the event of Herpes labialis. Said matrix is arranged on a flexible carrier film which is hydrophobic and also permeable to vapor.
US20050004105 Using serotonine receptor antagonist A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans using a 5-HT1A receptor agonist is provided.
CN101623273B Rifaximin medicament combination dispersible tablet and preparation method thereof The invention relates to a Rifaximin medicament combination dispersible tablet and a preparation method thereof. The medicament combination dispersible tablet comprises the following components by weight portion: 50-250 portions of Rifaximin, 10-150 portions of lactose, 50-160 portions of microcrystalline cellulose, 15-45 portions of partially substituted hydroxy propyl cellulose, 2-12 portions of acesulfame potassium, 15-45 portions of sodium carboxymethyl starch and 0.5-2.5 portions of magnesium stearte. Although the medicament combination dose not contain lauryl sodium sulfate as a cosolvent, the solubility property is favorable, and the dispersion property and the dissolution rate are both favorable. The preparation method of the medicament combination is simple to realize and is suitable for industrial production.
CN103006827A Sniffing medicine for treating tuberculosis and preparation method thereof The invention discloses a sniffing medicine for treating tuberculosis and a preparation method thereof. The sniffing medicine for treating tuberculosis disclosed by the invention comprises the following bulk pharmaceutical components in parts by weight: 1-2 parts of lead sulfate, 20-40 parts of calomel, 20-40 parts of vermilion, 40-80 parts of croton seeds and 300-600 parts of red jujubes. The preparation method of the sniffing medicine for treating tuberculosis disclosed by the invention comprises the following steps: removing pits of the red jujubes, and then sequentially placing the croton seeds, the lead sulfate, the calomel and vermilion in parts by weight in the red jujubes; then, wrapping the red jujubes three layers by using cabbage leaves, and roasting the obtained product 15-30 minutes by using charcoal fire; and finally, removing the cabbage leaves, and grinding the red jujubes into paste. The effect of the sniffing medicine on treating diseases such as tuberculosis and the like is obvious. The sniffing medicine is taken orally, and does not hurt the stomach, intestines, the liver and the kidney; and the sniffing medicine treats liver complaints, and the sniffing medicine directly reaches the lungs and enters the blood circulation so as to achieve effects of toxic substance counteracting, sterilization and parasite control.
CN1634008A Compound metformin hydrochloride xylitol oral preparation and its production method The invention provides a compound oral preparation for treating type II diabetes which comprises the components of metformin hydrochloride and xylitol by the weight ratio of 1-99 : 99-1. The oral administration preparation can be prepared into the dosage types of oral liquid or tablet. The invention provides a compound preparation prepared by utilizing oral antihypelipidemic medication of different mechanisms.
EP1446381B1 Anthranilic acid amides and pharmaceutical use thereof The invention relates to anthranilic acid amide derivatives of formula (I), wherein Ar is represented by the subformula (Ia), wherein Ra represents H or lower alkyl, and R1 represents H or perfluoro lower alkyl, R2 represents H, halogen, C2-C7alkyl, C2-C7alkenyl or lower aklynyl; or Ar is represented by the subformula (Ib) and R1 represents perfluoro lower alkyl, and R2 represents bromo, iodo, C2-C7alkyl, C2-C7alkenyl or lower alkynyl, or R1 represents H, and R2 represents fluoro, bromo, iodo, ethyl, C5-C7alkyl, C2-C7alkenyl or lower alkynyl; to N-oxides and tautomers thereof, and to salts of such anthranilic acid amides, its N-oxides and tautomers; to processes for their preparation; to their application in the treatment of the human or animal body, to the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age-related macular degeneration; to a method for the treatment of such diseases in animals; and to the use of such a compound - alone or in combination with one or more other pharmaceutically active compounds - for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.
US20090176794 1h-indol-1-yl-urea compounds Compounds of formula (I): wherein: R1 and R2, which may be the same or different, represent a hydrogen atom or a linear or branched (C1-C6)alkyl group, R3 represents a hydrogen or halogen atom, a linear or branched (C1-C6)alkyl group, or a linear or branched (C1-C6)alkoxy group, Het represents a pyridyl, pyrimidinyl or piperidyl group, which are optionally substituted by one or more groups selected from halogen, linear or branched (C1-C6)alkyl and linear or branched (C1-C6)alkoxy, —represents a single bond or a double bond, their enantiomers and diastereoisomers, and also addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of depression, anxiety, disorders of memory in the course of aging and/or neurodegenerative diseases, and in the palliative treatment of Parkinson's disease, and for adaptation to stress.
US20120010159 Combination therapies with cox-2 inhibitors and treprostinil The present invention is directed to compositions and methods for pain management, and for treating inflammation or an inflammation-associated disorder in a subject comprising administering to the subject a therapeutically effective amount of a COX-2 inhibitor and a therapeutically effective amount of a prostacyclin analog, such as treprostinil, a pharmaceutically acceptable salt thereof, or a treprostinil derivative described herein.
US20100160332 a2-Adrenoceptor Ligands The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into α and β subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel compounds which are ligands of the alpha2-adrenoceptor (α2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of α2-ARs associated disorders, such as depression and schizophrenia.
US7432252 Method of promoting cervical and vaginal secretions The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y2 and/or P2Y4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable agonists such as UTP, CTP, ATP, dinucleotides and analogs thereof are disclosed.
CN1785985A Demethyl sodium cartharidate medicinal compound and its preparation method and application The present invention discloses a disodium norcantharidinate medicine compound, its preparation method and application. Its molecular formula is C8H8O5Na2, and its molecular weight is 230.2. Said medicine is obtained by using 1 mol of norcantharidin and 2.0-2.5 mol of sodium hydroxide, making them be completely reacted at 2 deg.C-100deg.C, then making evaporation at 100deg.C-200deg.C to remove water content. Said invention also provides the application of said disodium norcantharidinate medicine compound in preparation of medicine for resisting tumor. It can be made into powder injection, liquid injection or transfusion preparation.
WO2008089669A1 A novel combination of epimedium-derived-flavonoids-fractions for prevention of steroid-induced osteonecrosis The present invention relates to novel pharmaceutical compositions comprising Epimedium wushanense Ying extracts, their methods of preparation, and their use in inhibiting thrombosis and lipid deposition. Also provided by the present invention is a method of preventing or treating steroid-associated osteonecrosis with the use of the pharmaceutical composition of the present invention. The preparation method of the present invention is stable and provides reproducible results, both in small scale extraction and large scale extraction.
EP0866691B2 Sublingual and buccal administration of selegiline The present invention is directed to improved methods for treating certain selegiline-responsive diseases or conditions and, more specifically, to methods in which selegiline is administered buccally or sublingually. Selegiline may be used either as a free base or as a pharmaceutically acceptable acid addition salt. The selegiline-responsive diseases or conditions include neuronal-degenerative diseases and conditions, such as Alzheimer's disease and neuronal damage from hypoxia, stroke, ischemia, and trauma, and dopaminergic-related, selegiline responsive diseases and conditions such as depression and ADHD.
US6906082 Cholesteryl ester transfer protein inhibitor; anticholesterol agents, cardiovascular disorders; synergistic mixture Cholesteryl ster transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
EP1648445B1 Indol-5-yl sulfonamide derivatives, their preparation and their use 5-ht-6 as modulators The present invention refers to new sulfonamide derivatives, of general formula (1a, 1b, 1c) optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or their salts, preferably the corresponding, physiologically acceptable salts, or corresponding solvates; to the processes for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them.
CN101010276B Novel cyclohexane derivative, prodrug thereof and salt thereof, and therapeutic agent containing the same for diabetes A cyclohexane derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity, metabolic stability, and safety; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, e.g., insulin dependent diabetes mellitus (type 1 diabetes) or noninsulin-dependent diabetes mellitus (type 2 diabetes), complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): (wherein A is -O-, -CH2-, or -NH-; nis an integer selected between 0 and 1; R6and R7 each independently is hydrogen or C1-6 alkyl; m is an integer selected among 1-3; Q is selected among the following formulae Q1 to Q5; Ar1 is optionally substituted arylene or optionally substituted heteroarylene, provided that the heteroarylene may be bonded to an aromatic carbocycle or aromatic heterocycle to form a fused ring; and Ar2 is optionally substituted aryl or optionally substituted heteroaryl), a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, or the like each containing the compound.
EP1930420A1 Isolated nucleic acid molecules encoding a bacterial uracil phosphoribosyl-transferase enzyme, cells transformed therewith and uses thereof Disclosed herein are novel polynucleotides encoding a uracil phosphoribosyl transferase, each being derived from Salmonella typhimurium. The disclosed uracil phosphoribosyl transferase protein is useful in sensitizing human cancer cells to treatment with anti-cancer agents such as 5-Fluorouracil.
US20080275006 Process for the Preparation and Isolation of Phosphatides Process for the preparation of phosphatidylserine of formula wherein R1 and R2 independently represent a saturated, mono-unsaturated or polyunsaturated acyl C10-C30, X═OH or OM where M=alkaline or alkaline earth metal, ammonium, alkylammonium (including the inner salt) including the transphosphatidylation reaction between phosphatidylcholine of the general formula wherein R1 and R2 and X have the above specified meanings, R3═CH2—CH2—NH2 o CH2—CH2—N+(CH3)3 and Serine in D, L or racemic form catalysed by the phospholipase D enzyme (PLD), characterised in that said reaction is carried out in a hydroalcoholic medium containing an aliphatic alcohol and in the presence of bivalent metal oxide.
EP2324041A2 Phosphonated rifamycins and uses thereof for the prevention and treatment of bone and joint infections The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
US20110152240 Pyrazolopyrimidines and related heterocycles as ck2 inhibitors The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and have the following general formula:
WO2006123674A1 Angiogenesis inhibitor containing amine derivative as active ingredient An object of the invention is to provide an angiogenesis inhibitor. The angiogenesis inhibitor of the invention contains a compound represented by the following general formula [I] or a salt thereof as an active ingredient. In the formula, the ring A represents a benzene ring or a naphthalene ring; X represents a single bond, an alkylene group or -CH2COOCH2-; Y represents an oxygen atom or N(R6); R1, R2 and R3 are the same or different and represent a hydrogen atom or an alkyl group, or R1 and R3 may be joined together to form a ring having one or more double bonds; R4 and R5 are the same or different and represent a hydrogen atom or an alkyl group; and R6 represents a hydrogen atom or an alkyl group.
WO2013127267A1 Pyridinyl and pyrimidinyl sulfoxide and sulfone derivatives Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
US20110009406 Tetrahydro-1h-pyrrolo fused pyridones The present invention relates to tetrahydro-1H-pyrrolo fused pyridone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
CN101298433A 2-, 3-, 4-, or 5-substituted-n1-(benzensulfonyl)indoles and their use in therapy The invention provides 2, 3-, 4- or 5-substituted-N1-(benzensulfonyl)indoles compounds of the general formula (I) in which Ar, R<2>, R<3>, R<4> and R<5> are as defined in the specification. The said compounds have affinity for the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders relating to the said receptor, such as obesity and CNS disorders.
US20120045519 Use of deoxyelephantopin (det) and analogues thereof for treatment of melanoma Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.
US8273765 Bicyclo-pyrazoles and pharmaceutical compositions comprising them Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.
EP1551792A1 Novel beta mimetics with extended duration of action, method for production and use thereof as medicaments The invention relates to compounds of general formula (I), where the groups R1, R2 and R3 can have the meanings given in the claims and the description, method for production and use thereof as medicaments, in particular for the treatment of inflammatory and obstructive bronchial diseases.
CN103330711A Flucloxacillin sodium and amoxicillin sodium for injection The invention relates to flucloxacillin sodium and amoxicillin sodium for injection, in particular to a stable flucloxacillin sodium and amoxicillin sodium pharmaceutical composition for injection. The composition comprises flucloxacillin sodium and amoxicillin sodium, wherein flucloxacillin sodium is counted as flucloxacillin, amoxicillin sodium is counted as amoxicillin; and the weight ratio of flucloxacillin to amoxicillin is 1:(0.5-1.5). The pharmaceutical composition has an excellent pharmaceutical performance.
US20060189530 Neuropeptide Y receptor Y5 and nucleic acid sequences The present invention provides novel NPY/PYY receptor proteins and the nucleic acid sequence encoding them. The invention is directed to the isolation, characterization, and pharmacological use of these receptors and nucleic acids. In particular, this invention provides human and rat NPY/PYY receptors (which we call the NPY Y5 receptor) and nucleic acids. Also provided are recombinant expression constructs useful for transfecting cells and expressing the protein in vitro and in vivo. The invention further provides methods for detecting expression levels of the protein as well as methods for screening for receptor antagonists and agonists to be used for the treatment of obesity or anorexia, respectively.
CN103127076A Application of Aphanamixoid A to lung cancer treatment medicine The invention discloses application of Aphanamixoid A to lung cancer treatment medicine and belongs to the technical field of novel application of medicine. The compound has good lung cancer resistance activity and can be used for preparing the lung cancer resistance medicine. The Aphanamixoid A can significantly inhibit non-small cell lung cancer cells A 549, giant-cell lung cancer cells NCI-H460, lung squamous carcinoma cells HTB-8 and human lung pavement epithelium cancer cells QG-5, wherein the non-small cell lung cancer cells A 549, the giant-cell lung cancer cells NCI-H460, the lung squamous carcinoma cells HTB-8 and the human lung pavement epithelium cancer cells QG-5 are cultured in vitro; the inhibiting effect of the Aphanamixoid A on normal human hepatic cells LO2 and peripheral blood lymphocyte is small, and therefore obvious selectivity is achieved. The application of the Aphanamixoid A to preparation of the lung cancer treatment medicine is made public for the first time. The skeleton type is fully novel, and inhibitory activity to the lung cancer cells is surprisingly strong.
WO2012065384A1 Tromantadine compounds with adamantane structure, derivatives and analogs thereof, and their uses as anti-tumor pharmaceuticals Disclosed are pharmaceutical compound tromantadine of the following formula (I), derivatives and analogs thereof, and their uses as anti-tumor pharmaceuticals. The present compounds can be used solely or in combination with other known anti-tumor pharmaceuticals for the treatment of tumor-relating diseases, or in combination with other known pharmaceuticals for the treatment of other diseases associated with concomitant tumor diseases, such as viral, mycotic and bacterial caused diseases, neurological diseases, emdorcine system diseases, immune system diseases, etc.
CN101843593A Novel vecuronium bromide freeze-dried preparation and preparation method thereof The invention discloses a novel vecuronium bromide freeze-dried preparation and a preparation method thereof. The novel preparation comprises the main components of vecuronium bromide, a freeze-dried excipient, polyethylene glycol playing a role in re-dissolving assistance, vitamin E playing a role in anti-oxidation, and glycerol serving as an isotonic regulator. According to the formula, the vecuronium bromide is developed into the novel freeze-dried preparation, and the process is simple. The novel vecuronium bromide freeze-dried preparation can improve the pH value of re-dissolved preparation solution to make the pH value reach or be close to the physiological pH range of blood, avoids or reduces stimulations caused by the preparation to a blood vessel, alleviates injection pains, and simultaneously can ensure that a medicament compound is fully dissolved to prevent insoluble substances from causing side effect injuries to a body.
CN101310722A New formulation of levamisole for treating asthmatia The invention relates to the preparation and the usage of a spraying agent, an aerosol, a powder inhalation and an inhalation of levamisole. The invention relates to the usage of the spraying agent, the aerosol, the powder inhalation and the inhalation of the levamisole for treating asthma.
CN1943616A Medicinal composition for treating impetigo herpetifomis The invention relates to a composition of medicines for treatment of skin disease, specifically speaking a composition of medicines for treatment of crusted tetter. Said composition consists of rosin, alum, soybean, sesame oil as materials, just mixing and shaking up directly and then ready for use.
CN101062233A Powdered medicine for coaptation and its preparing process The invention discloses a bone-knitting powder which is prepared from the following raw materials (by weight portions): ledebouriella root 6-14 parts, root of Dahurain angelica 10-20 parts, Japanese yam 10-30 parts, safflower 2-8 parts, notopterygium root 10-20 parts, levisticum 10-20 parts, Eupolyphaga Sinensis Walker 5-10 parts, Siphonostegia chinensis Benth 10-15 parts, notoginseng 5-15 parts, frank incense 5-15 parts, myrrh 4-15 parts and native copper 5-15 parts.
WO2011013359A1 Medicinal composition for iontophoresis Disclosed is a medicinal composition for iontophoresis, in which a medicinal agent has excellent stability, and which can be prepared and filled readily in the production process and can be produced at low cost. The medicinal composition for iontophoresis is characterized by comprising a nonionic synthetic polymer, betamethasone sodium phosphate, and a solvent. A preferred embodiment of the medicinal composition is characterized in that the nonionic synthetic polymer substance is polyvinyl alcohol (PVA). A preferred embodiment of the medicinal composition is characterized in that the content of polyvinyl alcohol (PVA) is 0.5 to 30 wt%.
CN101683315A Preparation method of composite hyaluronic acid-sulfadiazine silver gel The invention provides a preparation method of composite hyaluronic acid-sulfadiazine silver gel. The preparation comprises hyaluronic acid and sulfadiazine silver and the preparation is prepared by dissolving hyaluronic acid at high temperature and adding the dissolved hyaluronic acid in sulfadiazine silver. The composite hyaluronic acid-sulfadiazine silver gel of the invention has good biocompatibility and long half-life, thus being applicable to all kinds of antipyrotic and antibacterial situations.
EP2336132A1 Morpholinopurine derivative There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: wherein R1, R2, R3, R4, Ra, Rb, Rc, and X each have the same meanings as defined in the specification.
CN101590056A Application of N-[(2,3-di-2-furoquinoline-6-yl)amino]-(dimethylamino)-methanol in preparing anti-AIDS medicaments The invention belongs to the field of biological medicines, and in particular relates to application of a micromolecule compound with anti-HIV actively in preparing anti-AIDS medicaments. The invention provides application of N-[(2,3-di-2-furoquinoline-6-yl)amino]-(dimethylamino)-methanol in preparing the anti-HIV medicaments. The compound can inhibit CypA actively, the enzyme activity inhibition IC50 value (micron) reaches 3.47 +/- 0.92, and the compound has obvious inhibition to p24 protein of HIV-1 virus. The N-[(2,3-di-2-furoquinoline-6-yl)amino]-(dimethylamino)-methanol added to solution containing HIV can inhibit the replication of the HIV. The compound has the ability of inhibiting the replication of the HIV-1 virus, is a medicament designed aiming at a cell target, is not easy to form drug tolerance, and is suitable for the requirement on lifelong medication of AIDS patients.
EP1679301A1 Esters of nonsteroidal anti-inflammatory drugs and methods of their preparation Novel esters of nonsteroidal anti-inflammatory drugs with oligomers of 3-hydroxybutyric acid of the invention possess the general formula 1, where n from 2 to 35, and R is a radical of a non-steroidal anti-inflammatory drug selected from the group consisting of ibuprofen, ketoprofen, fenoprofen, naproxen, diclofenac, indomethacine, sulindac, tolmetin or salicylic acid. The method of preparation of compounds of the formula 1 consists in converting nonsteroidal anti-inflammatory drugs into a monosodium or monopotassium salts in the presence of a strongly polar solvent, preferably dimethyl sulfoxide (DMSO) or dimethylformamide (DMF), and in subjecting the obtained salts to the reaction with β-butyrolactone to open the lactone ring and to polymerize the lactone. The esters of the invention contain a nonsteroidal anti-inflammatory drugs bonded by means of an ester bond with oligomers of 3-hydroxybutyric acid including 2-35 mers as constituting biocompatible polymer carriers.
US20120100103 In situ forming hydrogel and biomedical use thereof Disclosed are in situ-forming injectable hydrogel and medical uses thereof. In the in situ-forming injectable hydrogel two or more homogeneous or heterogeneous polymers are bonded to each other by a dehydrogenation reaction between phenol or aniline moieties on adjacent polymers, wherein a polymer backbone is grafted with a phenol or aniline moiety using a linker. In contrast to conventional hydrogel, the in situ-forming injectable hydrogel is superior in terms of in vivo stability and mechanical strength thanks to the introduction of a water-soluble polymer as a linker which leads to an improvement in the reactivity of phenol or aniline moieties. Having the advantage of superior bio stability and mechanical strength, the hydrogel finds a variety of applications in the biomedical field.
CN102389428A Application of ligustrazine in preparing medicament for treating or preventing chronic anoxic bulbar injury The invention discloses application of ligustrazine in preparing a medicament for treating or preventing chronic anoxic bulbar injury. Experiments prove that: when the ligustrazine is applied to a chronic anoxic rat, neuron swelling of pre-Botc (pre-Botzinger complex), Amb (ambiguus nucleus), NTS (nucleus tractus solitarius), FN (facial nucleus) and 12N (hypoglossal nucleus) of medulla oblongata of the rat is reduced, and Nissl staining is darker than that of an anoxic group; the bulbar oxidative injury is lightened, and the oxidative injury resistance is reinforced, namely the content of lipid peroxide malonydialdehyde (MDA) is reduced, and the activity of superoxide dismutase (SOD) is increased; and the bulbar apoptosis resistance is improved, which indicates that the expression level of mRNA (messenger ribonucleic acid) of a bulbar apoptosis-resistance gene Bcl-2 (B-cell leukemia/lymphoma 2) is raised.
CN102058814B General flavone extractive of four medicaments including grassleaf sweetflag rhizome and preparation method thereof The invention provides a method for preparing and detecting a general flavone extractive of four medicaments including grassleaf sweetflag rhizome. The general flavone extractive of four medicaments including grassleaf sweetflag rhizome is prepared from the following raw medicinal materials in parts by weight: 200-600 parts of galangal, 100-300 parts of purpurea halitum, 50-150 parts of elecampane and 50-150 parts of grassleaf sweetflag rhizome. The preparation method of the general flavone extractive from the four medicaments including the grassleaf sweetflag rhizome can be prepared by adopting any one of the following methods or any combination of the methods: (1) a solvent extraction method; (2) a macroporous absorption resin method; (3) a polyamide method; and (4) a supercritical CO2 fluid extraction method, wherein the preferable methods include the macroporous absorption resin method and the polyamide chromatography method.
US20110124589 Inhaled fosfomycin/tobramycin for the treatment of chronic obstructive pulmonary disease The present invention provides the use of an aerosol formulation comprising fosfomycin and tobramycin in the treatment of patients with chronic obstructive pulmonary disease (COPD) who are experiencing or are at risk of experiencing acute exacerbations of COPD. Formulations for such use and methods of treating humans with COPD are also provided.
US20080119558 Drug for Inhibiting Production of Matrix Metalloprotease-9 A drug for inhibiting the production of matrix metalloproteinase-9 which contains leptomycin B or its derivative as the active ingredient can specifically inhibit the production of MMP-9 compared with MMP-2, furthermore, has an effect of inhibiting the production of MMP-9 even under stimulating the differentiation by adding calcium at a high concentration or adding TGF-β, and under stimulating for inducing inflammation by adding TNF-α or adding IL-2α.
US20110123501 Gut flora and weight management The present invention relates to supporting weight management, weight loss and/or to the prevention and/or treatment of metabolic disorders. In particular the present invention relates to preventing and/or treating metabolic disorders by modulating, in particular reducing the amount of proteobacteria and/or deferribacteres in the gut. One embodiment of the present invention relates to the use of a primary composition comprising an agent that reduces the amount of proteobacteria, preferably gamma-proteobacteria, even more preferred enterobacteria; and/or deferribacteres in the gut for the preparation of a composition to treat or prevent metabolic disorders, to support weight loss and/or to support weight management.
US20070269488 Hydrogel Nanocompsites for Ophthalmic Applications The present invention relates to reversible hydrogel systems. Particularly, the hydrogel of the present invention is made up of copolymers that can be a hydrogel when in an oxidized state and can be a solution when in a reduced state. A solution of the copolymer can be oxidized to form a hydrogel; and the hydrogel can be reduced to form a solution of the copolymer. Reversible nanogels can also be formed from a dilute solution of the copolymers. The hydrogel is formed with nanoparticles embedded therein to form a nanocomposite whose refractive index and modulus can be controlled by varying the amounts of nanoparticles and the polymer concentration of the hydrogel, respectively
EP0831769B2 Novel uses for thyroid hormones or thyroid hormone-like compounds This invention relates to the use of topically applied thyroid hormones and thyroid hormone-like compounds which are receptor binding ligands, either agonists or antagonists, to improve the appearance of the skin and underlying subcutaneous fat and improve certain medical conditions when applied topically. These compounds can be used to treat skin conditions such as stria, cellulite, roughened skin, actinic skin damage, intrinsically aged skin, photodamaged skin, lichen planus, ichthyosis, acne, psoriasis, wrinkled skin, and to diminish the size and improve the appearance of skin scarring from surgical or naturally occurring wounds, and to reduce the incidence of hyperkeratotic scarring. These hormones or hormone analogs will also increase the rate of epithelialization and collagen production. The thyroid agonists and antagonists may also promote differentiation and amelioration of dedifferentiated skin in premalignant lesions. The thyroid agonists and antagonists can be active in all organisms which contain the thyroid hormone receptors, notably amphibians, birds and subjects. Combination with Vitamin D analogs glucocorticoid and retinoids will potentiateand modify the effects of the thyroid hormones for increased benefit. Side effects of thyroid hormones which occur when the hormone is given orally and prevent usefulness for the above conditions are prevented when the hormone is topically applied.
US20090143464 Method for preventing and/or treating peripheral Neuropathies induced by the administration of an anticancer agent A method for preventing and/or treating peripheral neuropathies induced by the administration of an anticancer agent of the family of platin compounds, taxanes, epothilone class, vinca alkaloids, said method comprising the administration in a co-ordinated manner to a subject suffering from said peripheral neuropathies, or expected to suffer from said peripheral neuropathies, an effective amount of acetyl L-carnitine or of a pharmaceutically acceptable salt thereof. In case of prevention, acetyl L-carnitine is administered to a subject, in view of the need of a treatment with an anticancer agent, immediately before or immediately after surgical removal of the tumor, but in any case before the administration of the anticancer agent. Acetyl L-carnitine can enhance the supportive effect of physiological NGF during chemotherapy-induced neuropathy, thus avoiding the problem of the local and general side effects of the exogenous administration of NGF which are a major problem of this neuroprotective strategy.
US8445237 RNA interference mediating small RNA molecules Double-stranded RNA (dsRNA) induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). Using a Drosophila in vitro system, we demonstrate that 19-23 nt short RNA fragments are the sequence-specific mediators of RNAi. The short interfering RNAs (siRNAs) are generated by an RNase III-like processing reaction from long dsRNA. Chemically synthesized siRNA duplexes with overhanging 3′ ends mediate efficient target RNA cleavage in the lysate, and the cleavage site is located near the center of the region spanned by the guiding siRNA. Furthermore, we provide evidence that the direction of dsRNA processing determines whether sense or antisense target RNA can be cleaved by the produced siRNP complex.
US20080318964 Deuterium-enriched eszopiclone The present application describes deuterium-enriched eszopiclone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2008129308A2 Drug combination of beta 2 agonist and a progestin for the treatment of muscle loss The present invention is a product comprising a β2 agonist and a progestin, as a combined preparation for separate, simultaneous or sequential use in the treatment or prevention of muscle loss. The present invention is also a β2 agonist selected from R,R-formoterol, indacaterol or ritodrine, for use in the treatment or prevention of muscle loss.
WO2013173583A1 Psma inhibitors Compounds as defined herein are provided which are useful in (1) diagnostic methods for detecting and/or identifying cells presenting PSMA; and (2) methods for preparing the compounds.
CN102898523A N-substituted-tetrahydropyridylindole-monoclonal antibody CD14 conjugates, and preparation method and application thereof The invention discloses N-substituted-tetrahydropyridylindole-monoclonal antibody CD14 conjugates, and a preparation method and application thereof, belonging to the field of chemical biomedicine. The structure of the conjugates is disclosed as Formula (II): under the action of a condensing agent DCC, the amino acid residue at the C terminal in the CD14 monoclonal antibody molecule is combined with sec-amino group on the indole ring in N-substituted-tetrahydropyridylindole compounds (I) to obtain the monoclonal antibody CD14 conjugates with General Formula (II). The conjugates disclosed as Formula (II) can efficiently inhibit leukaemia K562 cell proliferation, and the IC50 value for inhibiting leukaemia K562 cell proliferation is obviously lower than that of the conventional chemotherapeutic drug 5-fluorouracil (5Fu); and the conjugates disclosed as Formula (II) have low toxicity for mouse normal marrow cells, and can be used for preparing drugs for treating leukaemia.
CA2107884C Use of vasoactive intestinal peptide (vip) to induce temporary paralysis of the gastrointestinal tract A method of inducing a temporary substantial paralysis of an area of interest in a patient undergoing a medical procedure is provided. The method involves administering a therapeutically effective amount of vasoactive intestinal peptide (VIP) admixed with a pharmaceutically acceptable carrier to a patient undergoing an endoscopy or other medical procedure.
EP2766008A1 Composition for nasal application with improved stability The invention relates to a pharmaceutical composition with improved stability for topical, particularly nasal, preferably intranasal application, to the use thereof, and to an application device containing said pharmaceutical composition.
WO2011088836A1 NOVEL 4-(ARYL-4-SULFONYL)-6,6a,7,8,9,10-HEXAHYDRO-4H-4,8,10a-TRIAZA-ACEPHENANTHRYLENE AND 3-ARYLSULFONYL-6,6a,7,8,9,10-HEXAHYDRO-3H-3,8,10a-TRIAZA-CYCLOPENTA[C]FLUORENE DERIVATIVES AS SEROTONIN 5-HT6 LIGANDS This invention is directed to compounds of formula I or II, which are serotonin 5-HT 6 ligands. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I or II, or a pharmaceutically acceptable salt thereof. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I or II, or a pharmaceutically acceptable salt thereof. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I or II, or a pharmaceutically acceptable salt thereof.
WO2012159446A1 METHOD FOR PRODUCING NATURAL β-CAROTENE BY FERMENTATION AND USE THEREOF Provided are a method for producing and purifying β-carotene by Blakeslea trispora fermentation and use thereof. The method comprises the following steps: a) separately inoculating the Blakeslea trispora strains onto a PDA culture medium so as to obtain a spore suspension; b) propagating spores in a seeding tank so as to obtain seeds for fermentation; c) inoculating the seeds for fermentation onto a fermenter and fermenting said seeds; d) by using an organic or inorganic base, adjusting the fermentation liquid to be basic, and filtering so as to obtain wet mycelia; e) treating the wet mycelia with a hydrophobic non-polar organic solvent; f) mixing the wet mycelia with an organic solvent of ester and obtaining a concentrated solution by extracting; g) adding a saturated monohydric alcohol into the concentrated solution, and filtering and crystallizing so as to obtain pure β-carotene. The content of the β-carotene in the present invention exceeds 96%, and the yield is above 81%.
WO2011119247A3 Topical skincare composition A composition and method for treating dermatological disorders (e.g., acne) is disclosed. In accordance with an embodiment, an antimicrobial composition includes a therapeutically effective amount of benzoyl peroxide and a therapeutically effective amount of hydrogen peroxide, where the combination of the benzoyl peroxide and hydrogen peroxide produces a synergistic effect, thereby enhancing the properties of both the benzoyl peroxide and hydrogen peroxide. In accordance with another embodiment, a skincare composition suitable for topical application to the skin includes from 1.0 to 10.0% by weight of benzoyl peroxide, and from 0.5 to 3.0% by weight of hydrogen peroxide, where the composition is substantially free of other therapeutic agents selected from the group consisting of anti-microbial agents, anti-bacterial agents, anti-viral agents, anti-fungal agents, and anti-inflammatory agents.
CN101732192A Macule-removing facial mask The invention relates to a macule-removing facial mask. The facial mask is prepared from 6-10 grams of hyacinth bletilla, 4-8 grams of excrementum passeris, 6-10 grams of aconitum fischeri peichb, 3-5 grams of galenite, 6-10 grams of angelica, 5-9 grams of almond and 5-20 grams of angelica. The materials of the facial mask belong to natural ingredients, and can directly permeate into the skin from the skin surface, thereby achieving the functions of cleaning, nursing and treatment and having the advantages of fast action and economy.
CN103110590A Cymipristone solid preparation and preparation method thereof The invention discloses a preparation method of a cymipristone solid preparation, which comprises the following steps: 1. dissolving cymipristone in a solvent to obtain a medicated solution, evenly mixing auxiliary materials with the medicated solution, and carrying out wet-process granulation, wherein the solvent is an organic solvent or a water solution containing more than 85 wt% of organic solvent; or 2. dissolving cymipristone in an acidifier-containing acidic solution to prepare a medicated acidic solution, evenly mixing auxiliary materials with the medicated acidic solution, and carrying out wet-process granulation. The invention also discloses a cymipristone solid preparation prepared by the method. The method disclosed by the invention avoids the defects of severe pollution, great loss and severe potential safety hazard caused by mechanical pulverization treatment, is simple to operate and easy to implement, has the advantage of high safety coefficient, and can be easily applied to industrial production. The cymipristone solid preparation prepared by the method has the advantages of excellent leaching property, high stability and high content uniformity.
CN100594903C HCV inhibiting bi-cyclic pyrimidines The present invention relates to the use of bi-cyclic pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinat ions of the present bi-cyclic pyrimidines with other anti-HCV agents.
WO2012060388A1 Organic amine salt of aminobenzoic acid derivative, and method for producing same The purpose of the invention is to provide a novel organic amine salt or quaternary ammonium salt of the 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino} benzoic acid represented by the formula shown below. The organic amine salt or quaternary ammonium salt has excellent pharmacokinetic characteristics and stability, and possessed properties useful for a drug.
US20120071492 Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.
US20100111893 Silicone Elastomer Exfoliating Compositions Compositions of the present invention comprise from about 40-99% of an aqueous suspension of silicone elastomer powder in a cosmetically acceptable vehicle. The compositions are useful as skin exfoliants when mechanical agitation is supplied, for example by rubbing with a hand. After exfoliation, little or no film or residue remains on the skin and washing the treated area is optional. The cosmetically acceptable vehicle may comprise a wide range of beneficial ingredients, cosmetic or dermatological actives and additives. The present invention also encompasses a method of exfoliating skin in need of such treatment.
WO2011095045A1 Pyridinone amide derivatives, preparation methods and medical uses thereof Provided are pyridinone amide derivatives, preparation methods and medical uses thereof. Particularly, novel pyridinone amide derivatives of formula (I) and pharmaceutical acceptable salts thereof, and uses thereof as therapeutic agents (especially as c-Met protein kinase inhibitors) are provided, wherein the substituents of formula (I) are defined as same as the description.
WO2014041784A1 Ube2t peptides and vaccines containing the same Peptide vaccines against cancer are described herein. In particular, epitope peptides derived from the UBE2T that elicit CTLs are provided. Isolated antigen-presenting cells with CTL inducibility and CTLs that target such peptides, as well as methods for inducing the antigen-presenting cell, or CTL are also provided. The present invention further provides pharmaceutical compositions containing such epitope peptides derived from UBE2T or polynucleotides encoding the polypeptides as active ingredients. Furthermore, the present invention provides methods for the treatment and/or prophylaxis of (i.e., preventing) cancers (tumors), and/or the prevention of a postoperative recurrence thereof, as well as methods for inducing CTLs, methods for inducing anti-tumor immunity, using the epitope peptides derived from UBE2T, polynucleotides encoding the peptides, or antigen-presenting cells presenting the peptides, or the pharmaceutical compositions of the present invention.
WO2014138806A1 Oxprenolol compositions for treating cancer The present invention relates to compositions of S-enantiomer enriched oxprenolol and their use in treating cancer and treating or preventing, in cancer patients, cachexia, body weight loss, lean body mass loss and adipose tissue loss, and improving quality of life and prolonging survival of cancer patients.
US7572886 Death associated proteins, and THAP1 and PAR4 pathways in apoptosis control The invention relates to genes and proteins of the THAP (THanatos (death)-Associated Protein) family comprising a THAP domain, and their use in diagnostics, treatment of disease, and in the identification of molecules for the treatment of disease. The invention also relates to the Par4 protein and SLC chemokine pathways, including the interaction of Par4 and SLC with THAP family proteins, and the recruitment and localization of Par4 to PML nuclear bodies.
US20120238511 2-deoxy-d-glucose formulations for prevention or treatment of neurodegenerative diseases Pharmaceutical compositions containing 2-deoxy-D-glucose (2-DG) and methods of use for promoting neurological health and prevention of age-related neurodegeneration, such as Alzheimer's disease (AD), have been developed. The compositions may be formulated such that the composition, or the compound when release from the composition, crosses the blood-brain-barrier and promote neurotrophism and neuroprotection mechanisms in the brain. 2-DG can be administered alone or in combination with one or more additional therapeutic, diagnostic, and/or prophylactic agents. The compositions described herein can be administered orally, enterally, transdermally, transmucosally, intranasally or parenterally, in a dosage effective to prevent or alleviate neuronal damage, effect neuronal regeneration or sustain viability, increase expression of anti-apoptotic proteins, and/or decrease indicators of Alzheimer's Disease. The formulations can be formulated for daily, sustained, delayed or weekly/monthly administration.
CN101422467A Immunosuppressant containing Withanolide type compound The invention discloses an immunosuppressor which containing a compound shown in the following general formula I and/or the general formula II, or an optical isomer thereof; wherein, R1, R2, R3, R4, R5, R6 and R7 are selected from H, OH, O-acyl, OMe, OEt, OPr, OPr, F, Cl, Br, NH2, NO2 or CN; wherein, site 5 and site 6 are an epoxy bond or a double bond; in the general formula I, the ether linkages of site 14 and site 27 are connected or disconnected; in the general formula II, the sites 14 and 15 and the sites 16 and 17 are the epoxy bond or the double bond, or a plant extract containing the compound. The immunosuppressor has stronger immuno-suppression effect, generates repression function to T and B lymphocyte periods which are excessively proliferated, and can be used for curing the self immunological diseases and relevant diseases.
CN103637998A Sustained-release tablet containing oxycodone and rotundine The invention relates to a sustained-release tablet containing oxycodone and rotundine, and particularly relates to a sustained-release tablet. The sustained-release tablet comprises (i) a slow release layer containing oxycodone or a medicinal salt thereof; (ii) a slow release layer containing rotundine or a medicinal salt thereof; (iii) a quick release layer containing oxycodone or the medicinal salt thereof and/or rotundine or the medicinal salt thereof. According to the method disclosed by the invention, a powerful analgesic compound preparation which is small in addiction and dependency is provided, and especially a powerful analgesic compound preparation, especially a sustained-release preparation which can prolong the drug release and/or is small in the addiction and/or the dependency is provided.
US7348350 Pyrazolyl biphenyl carboxamides and the use thereof for controlling undesirable microorganisms Novel pyrazolylbiphenylcarboxamides of the formula (I) in which R1, R2, X, m, Y and n are each as defined in the description, a plurality of processes for preparing these substances and their use for controlling undesirable microorganisms, and also novel intermediates and their preparation.
CN101632670B Suspension powder injection of piperacillin sodium and tazobactam sodium pharmaceutical composition and new application thereof The invention discloses a suspension powder injection of a piperacillin sodium and tazobactam sodium pharmaceutical composition, and further discloses an application thereof to preparing medicines for treating lung abscess.
DE102004003030A1 Composition containing a dihydroanthracene-disulfonic acid derivative, useful for treating inflammation of internal organs, e.g. ulcers, and cancer Pharmaceutical composition (A) that contains at least one dihydroanthracene-disulfonic acid derivative (I). - Pharmaceutical composition (A) that contains at least one dihydroanthracene-disulfonic acid derivative of formula (I). - R = hydrogen, (hydroxy)alkyl, ketone, aldehyde, ester or ether; - M = metal. - ACTIVITY - Antiinflammatory; Cytostatic; Hepatotropic; Nephrotropic; Antiulcer; Antiasthmatic. - No details of tests for these activities are given. - MECHANISM OF ACTION - None given.
EP1753742A2 Magnesium complexes of s-omeprazole The invention provides magnesium S-omeprazolato coordination compounds according to formula (I): [Mg(solva)x(solvb)y][Mg(S-omeprazolato)3]2•(solvc)z (I), pharmaceutical compositions and processes of making the same. In formula (I), solva, solvb, and solvc represent solvent molecules where x and y are independently selected from integers 0 to 6, the sum of which is 4 or 6, while z is a positive rational number from 0 to 6. The compounds are useful for the treatment of gastric acid related conditions and the inhibition of gastric acid secretion.
CN1948294A Amino acid diphenyl compound The present invention discloses an amino-acid diphenyl compound. Said compound is made up by using diphenyl, amino-acid and oxdiazole which are organically connected together. Said compound can be used for preparing the medicine capable of preventing and curing the disease of hypertension, coronary heart disease, angiocardiopathy, cerebrovascular disease, migraine and pulmonary hypertension, etc.
EP2305810A1 miRNAs in the treatment of fibrosis The present invention relates to nucleic acid molecules comprising at least ten contiguous bases having a sequence as shown in the sequence of miR-223 (SEQ ID NO: 16) for treating fibrosis. Also methods for treating fibrosis are provided.
US20080027107 With nitrogen containing heterocyclic substituents; for example, 1-{[(2-dimethylamino)ethyl]amino}-4-{[2-(3-hydroxypiperidin-1-yl)ethyl]amino}-anthracene-9,10-dione Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (Rs)2 in which R° is a C1l12 alkanediyl and each R5 is H or optionally substituted C14 alkyl, and a group of formula (11) in which at least one of R6,R7 and R8 is selected from X2 , and X2 substituted C1-4 alkyl and any others are H or C14 alkyl; R9 is selected from H, C14 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1.6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C16 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives. The amine compounds are cytotoxic and may be used as alkylating agents having topoisomerase II inhibiting activities in cancer therapy.
CN101732315A Method for preparing enrofloxacin microcapsules The invention discloses a method for preparing enrofloxacin microcapsules. The method uses ethylene cellulose as a capsule material, a plasticizer and an anti-sticking agent are also added in the preparation process, and the microcapsules are prepared by using a spray drying method. The preparation process has simple operation. The grain diameters of the microcapsules prepared by the method are small, the microcapsules with the grain diameters of 50 to 120mu m can reach over 50 percent, the microcapsules have smooth surfaces and good free-flowing property, and accessories can be added into the microcapsules to form oral preparation and injection. The oral preparation can be used for mixing with food for eating and mixing with water for drinking.
US20130029945 Darunavir Polymorph and Process for Preparation Thereof There is disclosed crystalline darunavir hydrate substantially free of any non-aqueous solvent.
US20080194564 the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.
WO2010043633A1 2h-pyrazolo [4,3-d]pyrimidin-5-amine derivatives as h4 histamine receptor antagonists for the treatment of allergic, immunological and inflammatory diseases Pyrazolopyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
WO2011074275A1 Skin barrier function promoter Disclosed are a preparation for external application and a preparation for internal application both of which are effective on the promotion of a skin barrier function. Also disclosed is a combination of the preparation for external application and the preparation for internal application. The preparation for external application and the preparation for internal application are characterized by comprising one or both of tocopherol and a glyceride represented by general formula (1) and astaxanthin. (In the formula, R1, R2 and R3 may be the same as or different from one another and independently represent a linear or branched saturated or unsaturated alkyl group having 8 to 22 carbon atoms.)
EP1915448A1 Nucleic acid agents for downregulating h19, and methods of using same Isolated oligonucleotides capable of down-regulating a level of H19 mRNA in cancer cells are disclosed. Articles of manufacture comprising agents capable of downregulating H19 mRNA in combination with an additional anti-cancer treatment are disclosed as well as methods of treating cancer by administering same.
CN101375852A Boletic acid quetiapine oral preparation and preparation method thereof The invention discloses a quetiapine fumarate oral preparation and a preparation method thereof. The quetiapine fumarate oral preparation is mainly prepared by raw materials with the following proportion by weight: 25-300 parts of quetiapine fumarate counted by quetiapine, 2-100 parts of disintegrating agent and 5-400 parts of filling agent. The preparation method of the oral preparation comprises the following process steps: (1) the quetiapine fumarate is taken, smashed, screened and evenly mixed with flavoring agent and the disintegrating agent, and wetting agent is added for preparing soft materials; (2) the soft materials are screen through a 20-mesh sieve for carrying out the granulation and the drying, the 20-mesh sieve is used for carrying out the size stabilization, the filling agent, an odor correcting agent, glidant and lubricant are added for even mixing; (3) the content of the drug which is evenly mixed is measured, the tablet weight is calculated, and the tablet pressing is carried out for the preparation. The oral preparation can be rapidly disintegrated in oral cavity without the use of water for the drug administration; the absorption is rapid and the bioavailability is high; and the taste is good.
US20110053970 Spirocyclic Cyclohexane Compounds Useful To Treat Substance Dependency Spirocyclic cyclohexane compounds useful in pharmaceutical compositions for use in the treatment of substance dependency.
CN103755652A Sulfonamide compound and application thereof The invention belongs to the technical field of medicines, and particularly relates to a sulfonamide compound and application thereof. The sulfonamide compound is as shown in formula (I) in the specification, an isomer of the compound as shown in formula (I) or a slat of the compound as shown in formula (I), wherein R is hydrogen, cyan, hydroxyl, halo-alkyl, alkoxy, alkoxy alkyl, alkylamino, alkylamino alkyl or R1; R1 is substituted carbonyl. Pharmacological activity screening results of the compound disclosed by the invention show that the compound has a good inhibiting effect on MCF-7 (human breast cancer cells) and HeLa (human cervical carcinoma cells), so the compound has good development and application prospects in anti-tumor aspect.
US6906092 Method of inhibiting matrix metalloproteinases The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
US7781487 N-(1-cyanocyclopropyl)-4,4-difluoro-2(S)-[2,2,2-trifluoro-1(S)-(4-fluorophenyl)ethylamino)octamide; rheumatoid arthritis, multiple sclerosis, myasthenia gravis, psoriasis, pemphigus vulgaris, Graves' disease, myasthenia gravis, lupus, asthma, pain, atherosclerosis; cathepsins B, K, L, F, and S inhibitors The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
WO2007079715A3 Novel lysolipin derivatives The invention relates to novel lysolipin derivatives, to uses of lysolipin derivatives of this type, to pharmaceutical compositions containing lysolipin derivatives of this type, to a method for producing said lysolipin derivatives and to intermediate products for producing lysolipin derivatives of this type.
US6991815 compositions which are effective in preventing and/or treating peptic ulcer diseases, comprising an effective amount of American ginseng and/or its extract The invention discloses a pharmaceutical composition for preventing and/or treating peptic ulcer, including American ginseng or the extract thereof, and a method for preparing American ginseng extract, said method including extracting American ginseng with water or ethanol aqueous solution, and then ultrafiltrating, dialyzing, precipitating with ethanol, or performing reverse phase chromatography to obtain various fractions of extract with anti-peptic ulcer effect.
CN101843626A Tincture for treating acne The invention relates to the technical field of medicine. The invention aims to provide a tincture medicament for treating acne, which has the advantages of convenient use, high compliance and good curative effect. Weisili acne tincture comprises metronidazole disodium hydrogen phosphate, salicylic acid, chloramphenicol and 75 percent alcohol. Clinical medicinal experiments prove that the tincture medicament is applicable to various types of acne such as erythemas, papulae, pustules, comedones, nodules cyst and the like, folliculitis, rosacea and the like and has the advantages of obvious curative effect, good safety and 95.12 percent of effective rate.
EP2045322A1 Double-muscling in mammals A gene (cDNA) encoding a bovine myostatin protein. The nucleic acid coding sequence is identified as SEQ ID NO:1 and the protein sequence is identified as SEQ ID NO:2. A mutant gene (SEQ ID NO:3) in which the coding sequence lacks an 11-base pair consecutive sequence (SEQ ID N0:11) of the sequence encoding bovine protein having myostatin activity has been sequenced. It has been shown that cattle of the Belgian Blue breed homozygous for the mutant gene lacking myostatin activity are double-muscled. A method for determining the presence of muscular hyperplasia in a mammal is described. The method includes obtaining a sample of material containing DNA from the mammal and ascertaining whether a sequence of the DNA encoding (a) a protein having biological activity of myostatin, is present, and whether a sequence of the DNA encoding (b) an allelic protein lacking the activity of (a), is present. The absence of (a) and the presence of (b) indicates the presence of muscular hyperplasia in the mammal.
US20100292300 Compositions and methods for inhibiting or reversing fibrotic disorders The present invention provides compositions and methods for inhibiting or reversing fibrotic disorders by administering a Hic-5 antagonist to a mammal in need thereof. The invention also includes methods for screening compounds to identify Hic-5 antagonists useful in inhibiting or reversing fibrotic disorders.
US20100239669 Combinations of statins and anti-obesity agent Co-therapy of an anti-obesity agent, a statin, is disclosed along with fixed combinations thereof. Atorvastatin and orlistat are preferred as the various components.
US7220750 Quinoline or quinazoline derivatives; antitumor agent, treating respiratory tract and gastrointestinal disorders The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
US20100015101 Novel tumor antigen peptides The invention relates to novel tumor antigen proteins and peptides derived therefrom and use of the same in the filed of cancer immunity. Specifically, the inventions relates to a peptide which comprises a partial peptide derived from Lengsin, BJ-TSA-9, C20orf42, BUB1, C10orf3 or HIFPH3 and is capable of binding to an HLA antigen and is recognized by a CTL, and a pharmaceutical composition comprising the peptide and a pharmaceutically acceptable carrier.
WO2012131717A3 2',3'-epoxypropyl-3.4-dihydroxy benzene and a process for the preparation thereof The present invention relates to a 2',3'-epoxypropyl-3,4-dihydroxy benzene as an anticancer agent and a process for the preparation thereof. Chemically, the epoxy compound is more stable because the labile allylic double bond was converted to epoxide. The ally lie double bond of 3,4- dihydroxyallylbenzene of the structure 1 has tendency to conjugate with the double bonds of the benzene ring. The 2',3'-epoxypropyl-3,4-Dihydroxy Benzene showed activity for the first time when tongue cancer cells (HSC-3) are being shown to be affected by epoxy hydroxychavicol. There was growth arrest as well as mortality of tongue cancer cells. Epoxy hydroxychavicol is consistent, stable and effective compound modified form of hydroxychavicol from betel leaf is the first time shown to be killing significantly the tongue cancer cells. Tongue cancer is one of the prevalent oral cancers in India and abroad where no remedy has yet been proposed.
CN103690527A Application of Aphanamgrandiol A to preparation of anti-helicobacter pylori medicaments The invention discloses an application of Aphanamgrandiol A to preparation of anti-helicobacter pylori medicaments. In-vitro activity experiments show that Aphanamgrandiol A has very strong anti-helicobacter pylori activity, is applicable to diseases of acute or chronic gastritis, gastric ulcer, duodenal ulcer, and the like, and thus can be used for preparing anti-helicobacter pylori medicaments. The application of the invention is disclosed for the first time, and has prominent substantive features and significant advance because of the strong activity of Aphanamgrandiol A.
EP1660068A4 Composition for treatment of tinea pedis and method of use A treatment for tenia pedis is provided for in a topical treatment. According to the invention, a method is provided for applying composition substances to the affected area, working the composition into the affected area, and removing the composition from the affected area. The composition comprises at least one ethoxylate and a sarcosinate. Alternatively, the ethoxylate can be exchanged for a methoxylate or a propoxylate. Acetylated lanolin alcohol, sodium lauroyl sarcosinate, EDTA, a foam stabilizer, a scrubbing agent, and water can also be added to the composition to assist performance.
CN103570728A Substituted pyrazolo[1,5-a]pyrimidine derivatives as well as preparation method and application thereof The invention relates to substituted pyrazolo[1,5-a]pyrimidine derivatives as well as a preparation method and application thereof, particularly relates to substituted pyrazolo[1,5-a]pyrimidine derivatives shown in the general formula I and pharmaceutically accepted salts thereof and also provides a preparation method of the compounds shown in the general formula I and an application of a composition containing one or more of the compounds to the preparation of drugs for treating and preventing human immunodeficiency virus (HIV) infection.
CN102093347A 1,3,6-trisubstituted-beta-carboline cyclin-dependent kinase 2 inhibitor and application thereof The invention relates to the field of pharmaceutical chemistry, in particular to 1,3,6-trisubstituted-beta-carboline alkaloids, a preparation method of the 1,3,6-trisubstituted-beta-carboline alkaloids, a pharmaceutical composition containing the compounds and medical application of the pharmaceutical composition containing the compounds. Especially, the invention relates to application of the 1,3,6-trisubstituted-beta-carboline alkaloids as cyclin-dependent kinase 2 inhibitors.
US7449448 Administering fructose of fructose containing oligosaccharide The present invention relates generally to a composition for use in the prophylaxis and/or treatment of one or more symptoms caused or exacerbated by consumption of alcohol which composition comprises: (1) fructose and (2) fructose-containing oligosaccharide.
US20110206780 Morphinan modulators of nmda receptors, sigma1 receptors, sigma2 receptors, and/or a3b4 nicotinic receptors The present invention relates to new morphinan modulators of NMDA receptors, σ1 receptors, σ2 receptors, and/or α3β4 nicotinic receptors, pharmaceutical compositions thereof, and methods of use thereof.
WO2007074073A1 Use of alkoxylates of monovalent and polyvalent alcohols or derivatives thereof as an antibiotic substitute in the feeding of animals The invention relates to the use of alkoxylates of monovalent and polyvalent alcohols or a derivative thereof as an antibiotic substitute in the rearing and keeping of livestock. The invention promotes increased weight gain and an improvement in the health of the animals.
CN102649765A Emodin di-n-octyl quaternary ammonium salt with anti-leukemia activity and preparation method thereof The invention discloses an emodin di-n-octyl quaternary ammonium salt with anti-leukemia activity and a preparation method thereof. The emodin di-n-octyl quaternary ammonium salt is methyl di-n-octyl-[2-(4,5-dihydroxyl-7-methoxyl-9,10-anthraquinonyl) methyl] ammonium salt. Experiments prove that an emodin derivative, i.e. the emodin di-n-octyl quaternary ammonium salt has proliferation inhibition effects of different degrees on four leukemia cell lines K562, NB4, U937 and Jurkat and can be used for preparing a medicament for treating leukemia. The emodin derivative methyl di-n-octyl-[2-(4,5-dihydroxyl-7-methoxyl-9,10-anthraquinonyl) methyl] ammonium bromide has the advantages of simple preparation process, mild preparation conditions and high yield of reaching up to over 50 percent; and in-vitro cancer cell inhibition experiments show that the four leukemia cell lines K562, NB4, U937 and Jurkat can be effectively killed off.
EP0910359B1 Selection and/or enhancement of resident microorganisms in the gastrointestinal tract Improved method of enhancing a population of one or more target microorganisms in the gastrointestinal tract of an animal, the improvement comprising providing to the animal a selected modified or unmodified resistant starch or mixtures thereof, such that the one or more microorganisms will selectively utilise the starch and/or increase in number and/or activity in the gastrointestinal tract, either uniformly throughout the gastrointestinal tract or at specific site or regions.
US6844306 Water-soluble, chlorhexidine-containing compositions and use thereof The invention relates to water-soluble, chlorhexidine-containing compositions having a long shelf life. The compositions are in the form of powder, granules or tablets and consist substantially of (i) a salt of chlorhexidine with 2 moles of a sugar acid and a microbicidally active quaternary ammonium bromide, or of (ii) chlorhexidine, a sugar acid or sugar lactone, with at least 2 moles of sugar acid or sugar lactone being present per mole of chlorhexidine, and a microbicidally active quaternary ammonium bromide. Peferred compositions consist substantially of chlorhexidine digluconate and N-cetyl-N,N,N-trimethylammonium bromide (cetrimide) in a weight ratio of 1:1 to 1:10. The solid compositions are stable, with little or no p-chloroaniline splitting off during storage.
CN101862296B Cefmetazole sodium composition powder injection for injection The invention relates to cefmetazole sodium composition sterile powder for injection, which comprises 99.0 to 99.9 weight percent of cefmetazole sodium and 0.1 to 1.0 percent of sodium benzoate. The cefmetazole sodium is cefmetazole sodium crystal and the primary granularity of the cefmetazole sodium ranges from 80 to 120 mu m. The cefmetazole sodium composition sterile powder for injection provided by the invention contains the cefmetazole sodium crystal, and has the advantages of large crystal granularity, uniform granularity distribution, qualified quality, and high stability.
CN101020655A Process of extracting 1-deoxy nojirimycin The present invention is process of extracting 1-deoxy nojirimycin (DNJ) from mulberry leaf. Mulberry leaf extract is treated with inorganic acid, cooled to eliminate impurity and column chromatographically separated to obtain DNJ. Animal experiment of mouse shows that the mulberry leaf extract has obvious blood sugar reducing effect, so that the present invention may be used in preparing blood sugar reducing health product. The present invention has low preparation cost, and is suitable for industrial production.
US20060014741 Synthetic process, and crystalline forms of a pyrrolotriazine compound The present invention provides a process for preparing pyrrolotriazine compounds of formula (I) or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of the pyrrolotriazine compound [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2, 1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester and pharmaceutical compositions comprising at least one crystalline form, as well of methods of using the crystalline forms in the treatment of a proliferative disease, and methods for obtaining such crystalline forms. The compounds of formula (I), including [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester, are useful for inhibiting tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
CN101235040B Phomopsis rhzomorph compound and its preparation method and application A phomopsis compound, a corresponding preparation method and an application relate to two compounds. The invention provides a phomopsis compound of sea weed fungus with strong antibacterial activity and application in antibacterial drugs, a corresponding preparation method and an application, wherein the sea weed fungus is hzla01-1(Phomopsis sp.hzla01-1) as phomopsis compound A and B, compound A is colorless oily substance, and the compound B is colorless acicular crystal. The preparation method comprises seed cultivation of phomopsis hzla01-1, fermentation of phomopsis hzla01-1, extraction ofphomopsis compound and refining phomopsis compound. Pharmacological verification proves that the compound has significant antibacterial function and can be used to prepare new antibacterial drug.
EP2243485A1 Anti-viral agents, anti-viral fibers and anti-viral fiber structures Provided are antiviral agents that are effective in inactivating viruses, and fiber products and fiber structures carrying these antiviral agents. The antiviral agent effectives against influenza and comprises a metal phthalocyanine derivative represented by formula I. Fiber carries these antiviral agents.
US20100166806 Combination therapy comprising the use of protein kinase C modulators and Histone Deacetylase inhibitors for treating HIV-1 latency The invention relates to a combination of treatments, more particularly a combination treatment for HIV-1 infection. The present invention is directed to the use of bryostatin-1 and their natural and synthetic derivatives for AIDS therapy, in particular to the use of bryostatins in combination with other active drugs such as Histone Deacetylases (HDACs) inhibitors and anti-retrovirals, for the treatment of HIV-1 latency. According to the present invention, we provide a combination therapy for the treatment of HIV-1 latency which employs bryostatin-1 (and analogues) and one of the following HDAC inhibitors; valproic acid, butyrate derivatives, hydroxamic acids and benzamides. While HDACi can be used in continuous dosing protocol, bryostatins can be used following a cyclical dosing protocol. Bryostatins can be formulated in pharmaceutical acceptable carriers including nanoparticles, phospholipids nanosomes and/or biodegradable polymer nanospheres. This combination therapy needs to be used in patients treated with antiretroviral therapy (HIV-1 protease inhibitors, HIV-1 reverse transcriptase inhibitors, HIV-1 integrase inhibitors, CCR5 co-receptor inhibitors and fusion inhibitors).
CN1762358A Moxifloxacin capsule and its preparation method The invention provides a Moxifloxacin capsule, which comprises Moxifloxacin or its salts and/or hydrate, at least a disintegrating agent and at least a lubricating agent, the shell of the capsule contains hydroxy propyl ethyl cellulose. The invention also discloses the process for preparing the capsule.
WO2008127725A1 Compositions and methods for treatment of psychiatric disorders Compositions and methods for the treatment of a unipolar depression containing betaine, and folate. Formulations for oral administration optionally also contain L-methionine.
CN102858744A Trypsin-like Serine Protease Inhibitors, And Their Preparation And Use The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.
DE102006012872A1 Agent, useful e.g. for the effective lowering of increased cholesterol levels in blood, comprises long-chain carboxylic acid on the basis of montana waxes and/or guerbet acid or the corresponding components of carnauba wax or shellack Agent for the effective lowering of increased cholesterol levels, comprises long chain carboxylic acid on the basis of montana waxes as well as their derivatives (VLCFA: very long-chained fatty acid) and/or guerbet acid or their derivatives or the corresponding components of carnauba wax or shellack, where the long chain carboxylic acids possess a chain length distribution of 14-40 carbons, preferably 28-40 carbons. - ACTIVITY : Antilipemic. - MECHANISM OF ACTION : None given.
CN103304424A Diisopropylamine dichloroacetate compound and compound medicine composition injection thereof The invention relates to a diisopropylamine dichloroacetate compound and a compound medicine composition injection of the diisopropylamine dichloroacetate compound. The diisopropylamine dichloroacetate compound is a crystal; the X-ray powder diffraction measurement of the compound proves that the characteristic peak at (2theta+/-0.2) in the pattern is displayed at 12.7 degrees, 13.8 degrees, 16.3 degrees, 16.9 degrees, 18.8 degrees, 24.4 degrees, 26.0 degrees, 29.2 degrees, 30.8 degrees, 32.2 degrees, and 32.9 degrees. The active ingredients of the compound medicine composition injection comprise the diisopropylamine dichloroacetate compound provided by the invention and sodium gluconate. Compared with the prior art, the compound diisopropylamine dichloroacetate composition lyophilized powder and injection, which take the diisopropylamine dichloroacetate compound provided by the invention as the active ingredient, are greatly improved in technical stability, and the sodium acetate added in the prescription of the injection can be used for further improving the stability.
US20060229335 Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a One aspect of the present invention relates to certain diarylamine and arylheteroarylamine pyrazole derivatives of Formula (A) and pharmaceutical compositions that modulate the activity of the human 5HT2A serotonin receptor. Compounds and pharmaceutical compositions are directed to methods useful in the prophylaxis or treatment of reducing platelet aggreagation, sleep disorders, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia and NOS schizophrenia and related disorders. Another aspect of the present invention is directed to the method of prophylaxis or treatment of 5HT2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.
WO2013131157A1 Combination of a monosubstituted sulfamate derivative of the natural monosaccharide d-fructose (topiramate) with an anti-depressant from the phenyl ketone class (bupropion) for treating obesity and plurimetabolic syndromes Combination of a monosubstituted sulfamate derivative of the natural monosaccharide d-fructose (topiramate) with an anti-depressant from the phenyl ketone class (bupropion) for treating obesity and plurimetabolic syndromes, which takes "combined therapy" into consideration, with the use of two drugs (topiramate and bupropion) with different mechanisms of action, with a view to promoting the synergistic effect thereof in reducing body weight. The solid pharmaceutical form contains 75 to 400 mg of bupropion hydrochloride combined with 25 to 200 mg of topiramate; excipients are added to the formulation to q.s. for 1 tablet/coated tablet.
CN103725536A Safflower health wine for myopia The invention relates to a safflower health wine for myopia. The wine is prepared by the following steps: cleaning and dry 20 g of safflower, 16 g of cassia twig, 12 g of radix paeoniae alba, 11 g of red ginseng, 16 g of dodder and 15 g of borneol; grinding the above raw materials into a powder, adding the power into an extraction tank, adding liquor of 48 degrees and in weight 5 times of the medicine, soaking for 15-30 days, and filtering to obtain a filtrate; and adding 3000 g of pure grain liquor into the filtrate, then sealing and storing for 1-3 months to obtain the safflower health wine for myopia. The safflower health wine for myopia has the advanategs of simple manufacturing method and convenience for drinking, has effects of nourishing yin, clearing heat, clearing liver and improving eyesight, and can help people nourish yin, clear liver, improve eyesight and relieved symptoms of myopia by frequent drinking.
US20080057510 Human Vascular IBP-Like Growth Factor A human Vascular IBP-Like Growth Factor polypeptide (VIGF) and DNA (RNA) encoding such polypeptide and a procedure for producing such polypeptide by recombinant techniques is disclosed. Also disclosed are methods for utilizing such polypeptide for wound healing or tissue regeneration, stimulating implant fixation and angiogenesis. Antagonist against such polypeptides and their use as a therapeutic to treat atherosclerosis, tumors and scarring are also disclosed. Diagnostic assays for identifying mutations in VIGF nucleic acid sequences and altered levels of the VIGF polypeptide are also disclosed.
US7563467 Use of an Opuntia ficus-indica extract and compounds isolated therefrom for protecting nerve cells An ethyl acetate extract of Opuntia ficus-indica and compounds isolated therefrom for preventing and treating brain diseases such as Alzheimer's disease, stroke and Parkinson's disease, cell and tissue damage caused by ischemia, or cardiovascular system disease such as myocardial infarction.
US7429614 Medicament containing an effector of the glutathione metabolism together with α-lipoic acid for treating diabetes mellitus The invention relates to a medicament containing an effector of the glutathione metabolism together with α-lipoic acid for treating diabetes mellitus. This medicament enables disturbances of the thiol-disulfide status or those that occur, for example, in diabetes mellitus to be treated simultaneously, separately or in a temporally graduated manner.
WO2012097683A1 Bicyclic inhibitors of alk The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
CA2263961C Cocaine receptor binding ligands The invention relates to novel compounds of formula (I): (see formula I) which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases.
US7977383 Containing alkali ions, electrolytes, a buffer, polyol, saccharide and hydroxamic acid derivatives Described is a protective solution for avoiding ischemic, storage or ischemia/reperfusion to organs, or to isolated cell systems, or to tissue components after perfusion, surgery, transplantation, or cryopreservation and subsequent reperfusion, which contains alkali ions, and if need be also alkaline earth ions as the electrolyte, a buffer e.g. on a histidine derivation basis, as well as a polyol and/or a saccharide, has an osmolarity of about 290 mosm/l to about 350 mosm/l, as well as a pH value of about 6.8 to about 7.4, and to which hydroxamic acid, and/or one or more hydroxamic acid derivatives are added.
CN1628644A Medicine for recurrent baby pig bowel oedema disease and preparation method thereof The invention provides a medicine for treating recurrent baby pig bowel oedema disease and preparation method, where the medicine is prepared from (by weight percent) borneol 1-3 parts, ethanol 5 parts, propylene glycol 1 part, distilled water 3 parts, or borax 1.5 part, starch 0.5 part to prepare tablet.
CN103462996A Application of Neonectrolide A in preparing medicament for treating acute renal failure The invention relates to novel medicine application of Neonectrolide A, namely application of Neonectrolide A in preparing a medicament for treating acute renal failure, which is disclosed for the first time. The frame model belongs to a brand-new frame model, and Neonectrolide A has a strong activity in inhibiting acute renal failure, has a highlighted substantial characteristic, and is remarkably progressed in resisting acute renal failure.
CN101152208A Application of brown seaweed polyoses sulfate in preparing medicament for treating senile dementia The invention provides a brown seaweed polysaccharide sulfate with the purpose of preventing and treating senile dementia. The brown seaweed polysaccharide sulfate of the invention can be natural polysaccharide extracts from brown algae like kelp, focus, asophyllum, laminaria japonica or chorda filum, etc, or low molecular weight sulfuric acid polysaccharide or oligosaccharide material prepared by degradation of brown seaweed polysaccharide sulfate. The product of the invention has high safety and can be taken for a long term.
CA2803448A1 Imidazopyridine, imidazopyrimidine and imidazopyrazine derivatives as melanocortin-4 receptor modulators Disclosed is a compound of Formula I or a salt thereof, in which X, X1, X2, R1, R2, and R3 are described herein. Also disclosed are pharmaceutical compositions and methods of using the compounds of Formula I to treat disorders mediated by melanocortin-4 receptors.
CN103446104A Applications of Sarcaboside B in medicament against helicobacter pylori The invention relates to applications of Sarcaboside B in a medicament against helicobacter pylori. In-vitro activity experiments show that the Sarcaboside B has strong activity against the Helicobacter pylori Hp. The Sarcaboside B can be used for treating diseases of acute and chronic gastritis, gastric ulcer, duodenal ulcer and the like, and can be applied to preparing medicaments for treating acute and chronic gastritis, gastric ulcer and duodenal ulcer. The applications of the Sarcaboside B in preparing the medicament against helicobacter pylori are disclosed for the first time. As a skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpectedly strong helicobacter pylori inhibition activity, and the possibility of giving any inspiration by other compounds does not exist. The Sarcaboside B has significantly substantive characteristics, as well as obviously prominent progress in the prevention and treatment of the helicobacter pylori infection.
EP2175879A1 Treatment of prion protein related diseases According to the present invention, treatment of prion protein related diseases, and in particular cancer tumours, is effected by providing to a subject in need thereof a therapeutically effective amount of an agent capable of modulating binding of a prion protein and/or a prion-like protein to a disease related GAG and/or HSPG.
US7410656 Isolated euphorbia plant compounds and derivatives; jatrophanes, pepluanes, paralianes, ingenanes; cytotoxicity against malignant melanomas and squamous cell carcinomas This invention relates to a compound or group of compounds present in an active principle derived from plants of species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, and to pharmaceutical compositions comprising these compounds. Extracts from these plants have been found to show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). In a preferred embodiment of the invention, the compound is selected from the group consisting of jatrophanes, pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable salts or esters thereof, and more particularly jatrophanes of Conformation II.
CN103751295A Externally-applied medical composition for treating swelling as well as externally-applied medicinal oil for treating swelling and preparation method of medicinal oil The invention discloses an externally-applied medical composition for treating swelling. The externally-applied medical composition is prepared from the following raw materials in parts by weight: 20-30 parts of herba menthae, 10-20 parts of folium isatidis, 10-15 parts of Chinese honeylocust fruit, 15-30 parts of Japanese milkwort herb, 5-15 parts of indigo naturalis, 10-20 parts of common cnidium fruit, 10-20 parts of rhodiola, 10-20 parts of fructus forsythiae, 2-10 parts of sodium chloride, 10-15 parts of fructus anisi stellati, 10-20 parts of radix glycyrrhizae and 20-50 parts of perfoliate knotweed herb. The invention further provides an externally-applied medicinal oil for treating swelling and a preparation method thereof. The externally-applied medicinal composition and the externally-applied medicinal oil have the benefits that the adopted raw materials are economical, a significant curative effect on swelling caused by bites of various insects, bees and ants is achieved, and the effect of relieving swelling and pain is achieved.
US20120027777 Ljungan virus with improved replication characteristics The present invention relates to a Ljungan virus with improved replication characteristic and the use of this Ljungan virus, amongst other thing, in the production of a vaccine.
US7452881 Such as N-[3-(2-diethylaminoethyl)-1H-indol-5-yl]-5-chloro-3-methylbenzo[b]thiophene-2-sulphonamide; serotonin receptors antagonist; anxiolytic, antidepressant, cognitive activator, senile dementia, psychosis, attention deficit/hyperactivity disorder The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.
US20070275922 RNAi-MEDIATED INHIBITION OF IGF1R FOR TREATMENT OF OCULAR ANGIOGENESIS RNA interference is provided for inhibition of IGF1R mRNA expression for treating patients with ocular angiogenesis, particularly for treating retinal edema, diabetic retinopathy, sequela associated with retinal ischemia, posterior segment neovascularization (PSNV), and neovascular glaucoma, and for treating patients at risk of developing such conditions.
US20120295853 Neuronal pain pathway The present invention relates to the discovery of a novel molecular pathway involved in long-term hyperexcitability of sensory neurons, which, in higher animals, is associated with persistent pain. It is based on the discovery that, following injury to an axon of a neuron, an increase in nitric oxide synthase activity results in increased nitric oxide production, which, in turn, activates guanylyl cyclase, thereby increasing levels of cGMP. Increased cGMP results in activation of protein kinase G (“PKG”), which then is retrogradely transported along the axon to the neuron cell body, where it phosphorylates MAPKerk.
WO2013140120A1 Glycerol solvate forms of (r) - 2 - [ [ [3 -methyl -4 (2,2, 2 - trifluoroethoxy) pyridin- 2 - yl] methyl] sulphinyl] - 1h - ben zimidazole The present invention relates to novel crystalline forms of (R)-2-[[[3-methyl-4(2,2,2- trifluoroethoxy)pyridin-2-yl]methyl]sulphinyl]-lH-benzimidazole (Formula 1), to processes for their preparation, to pharmaceutical compositions comprising the same and to the use of such crystalline forms for the treatment of gastrointestinal (GI) disorders.
CA2159610C Prodrugs with enhanced penetration into cells The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a human related to supranormal intracellular enzyme (e.g. phospholipase and/or esterase) activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound accumulates selectively within cells having such supranormal intracellular enzyme activity. Exemplary conjugates are esters of the carboxylic function in the formula, with e.g. heptanoyl-sn-3--glycerophosphoryl-choline or octanoyl-sn-3-glycerophosphoryl-choline.
EP2513112A2 Method for late introduction of the (8r)-hydroxyl group in carbapenem beta-lactam antibiotic synthesis The presently disclosed subject matter demonstrates that ThnG and ThnQ enzymes encoded by the thienamycin gene cluster in Streptomyces cattleya oxidize the C-2 and C-6 moieties of carbapenems, respectively. ThnQ stereospecifically hydroxylates PS-5 giving N-acetyl thienamycin. ThnG catalyzes sequential desaturation and sulfoxidation of PS-5, giving PS-7 and its sulfoxide. The ThnG and ThnQ enzymes are relatively substrate selective, but give rise to the oxidative diversity of carbapenems produced by S. cattleya, and orthologues likely function similarly in allied streptomyces.
US7141562 Central nervous system disorders; Parkinson's disease; Huntington's diseases; antidepressants; anxiolytic agents Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO2— or —(CRaRb)r—, n is 1 or 2, R2 is aryl or heteroaryl, and R1, R3, R4, R5, R6, R7, R8, R9, Ra, Rb, m, p, q and r, are as defined herein. The compounds are modulators of the 5-HT6 receptor and are useful for treatment of central nervous system disorders. Also provided are methods for preparing, compositions comprising, and methods for using Compounds of Formula I.
CN102247359A New application of 3,3'-bis(5-bromoindole) methane The invention belongs to the field of radiation injury protective medicaments, and relates to new application of 3,3'-bis(5-bromoindole) methane, namely application to the preparation of the radiation injury protective medicaments. A structural formula of the 3,3'-bis(5-bromoindole) methane is shown in the specifications. The 3,3'-bis(5-bromoindole) methane can be used for preparing the radiation injury protective medicaments and can improve the survival rate of cells subjected to ionizing radiation under the condition of low concentration without toxic or side effect.
US7589126 Useful as potent and selective activated blood coagulation factor X inhibitors, anticoagulants; for example, ethyl [4-[2-[2-hydroxy-5-(N-hydroxycarbamimidoyl)benzenesulfonyl-amino]ethyl]-2'-methanesulfonylbiphenyl-3-yloxy]acetate; brain and cardiovascular disorders The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.
CN103373986A Crizotinib prodrug, as well as preparation and application thereof The invention relates to a crizotinib prodrug, as well as a preparation and an application thereof. The invention provides a compound showed as a general formula (II) or a stereoisomer thereof, or a pharmaceutically acceptable salt, or a solvent compound or a hydrate of the compound, wherein X is O or CH2; m is 0 or 1; R1 and R2 are selected from the same or different groups, and are respectively independently hydrogen, halogen, nitryl, cyan, hydroxyl, amino saturated or unsaturated chain hydrocarbyl of C1-C6, and saturated or unsaturated cyclic hydrocarbyl of C1-C6; R1 and R2 also can exist in the same ring and form ternary-hexahydric ring together; the ternary-hexahydric ring can be substituted or un-substituted cyclic hydrocarbon, aromatic ring or hetero-aromatic ring; the substituent group on the ring can be selected from halogen, nitryl, cyan, hydroxyl, amino, C1-C6 alkyl and C1-C6 alkoxy; R3 is selected from hydrogen, substituted or un-substituted C1-C12 saturated or unsaturated alkyl, substituted or un-substituted phenyl or hetero-aryl, substituted or un-substituted alkyl acyloxy, substituted or un-substituted phosphorus acyloxy and substituted or un-substituted aryl acyloxy or hetero-aryl acyloxy; and the substituent groups are selected from halogen, nitryl, cyan, hydroxyl, amino, phenyl or hetero-aryl, C`-C6 alkyl, C1-C6 acyloxy, C1-C6 vinyl and C1-C6 alkynyl.
WO2009124460A1 Tripterygium wilfordii diterpene lactone derivatives, their pharmaceutical compositions and their application in inhibiting tumour of reproductive system The invention discloses Tripterygium wilfordii diterpene lactone derivatives represented by formula (1), their optical isomers and pharmaceutically acceptable salts and hydrates. The invention also provides pharmaceutical compositions and preparations comprising therapeutically effective Tripterygium wilfordii diterpene lactone derivatives represented by formula (1), their optical isomers and pharmaceutically acceptable salts and hydrates, and conventional pharmaceutical auxiliaries. The invention also discloses the application of the pharmaceutical compositions. The invention screens Tripterygium wilfordii diterpene lactone derivatives with good effect and low toxicity and makes them use in preparing medicaments for treating tumor diseases. The pharmaceutical compositions can be formulated to preparations in favor of the absorption by warm blood's tissues and apparatuses and have good application foreground in treating proliferative diseases such as tumors and so on.
CN1778305A Use of Pennogenin in preparing hemostatic medicines An application of the Piannuosaponin in preparing the staltic medicines for preventing and treating various hemorrhagic diseases, such as general hemorrhage, visceral hemorrhage, menorrhagia, etc, is disclosed.
US20100093680 Use of 3-alpha-androstanediol, optionally in combination with a 5-ht1a agonist, in the treatment of sexual dysfunction The invention relates to the field of male and/or female sexual dysfunction. The invention specifically relates to the use of 3-alpha-androstanediol, preferably in combination with a 5-HT1A agonist. Optionally, said 3-alpha-androstanediol and said 5HT1a agonist are further combined with a type 5 phosphodiesterase (PDE5) inhibitor.
WO2011045593A1 Novel macrocyles and methods for their production There are provided compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein the variables R1-R3 are as described in the description, said compounds being useful as anti-inflammatory agents with reduced systemic effects.
WO2009024348A1 Method for activating regulatory t-cells The invention relates to a method for activating regulatory t-cells (Treg-cells) of the human or animal body, comprising a step of bringing into contact the regulatory t-cells (Treg-cells) in a suitable liquid medium with one or a plurality of inhibitors of alanyl-amino peptidase (amino peptidase N; APN) and/or with one or a plurality of inhibitors of peptidases with the same substrate specification by induction of a suppressive effect of the regulatory t-cells (Treg-cells).
US20120245213 Human type i taste receptor subunit 3 modulators and methods of using same Methods and compositions are provided for modulating the activity of human type I taste receptor subunit 3 (hT1R3). Such materials and methods are useful for the screening and preparation of compositions and methods for the treatment of carbohydrate and lipid metabolic diseases and disorders.
US7674825 Cardiovascular disorders; stimulant of guanylate cyclase The present invention relates to the use of compounds of the formula (I) and to their salts and stereoisomers, for the preparation of medicaments for the treatment of cardiovascular disorders.
CN103599077A Freeze-dried powder of pravastatin sodium composition for injection The invention provides a freeze-dried powder of a pravastatin sodium composition for injection, and relates to the technical field of medicines and medicine production. The freeze-dried powder comprises the following raw materials by weight: 1 part of pravastatin sodium, 0.2-1.4 parts of chitosan nanoparticles and 100-200 parts of water for injection. The freeze-dried powder has the advantages that (1) chitosan, as a cosolvent, can increase solubility of pravastatin sodium in water and shorten dissolution time, and is helpful for clinical application; (2) the composition can significantly enhance a lipid-decreasing of pravastatin sodium, reduce usage amount of pravastatin sodium clinically and alleviate adverse effects of pravastatin sodium; in-vitro experiments demonstrate that the lipid-decreasing capacity of 10 mg of the freeze-dried powder of pravastatin sodium composition comprising the chitosan nanoparticles is equivalent to that of 20 mg of pravastatin sodium with no chitosan nanoparticles; and (3) chitosan nanoparticles can replace mannitol to be used as a freeze-drying skeleton agent, so that active effects of mannitol to a human body can be eliminated.
WO2011123042A1 Vaccination procedure and products for use therein A method of eliciting in a subject enhanced titres of antibodies specific for a selected hapten molecule, such as nicotine, which hapten molecule is included in at least two different hapten carrier conjugates is described. The method comprises the steps of initially immunizing the subject with one hapten carrier conjugate and subsequently booster immunizing the subject with at least one other hapten carrier conjugate. Products for use in said method. A hapten carrier conjugate vaccine combination comprising at least two different hapten carrier conjugate vaccines, one primary vaccine and at least one boost vaccine, as well as a commercial package containing them are also described.
US20090275574 Novel compounds-300 Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4, m, n, q, s, t, X, and Y are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
CN102920800A Topical drug composite and application and preparation method thereof The invention discloses a topical drug composite, and the formula comprises: by weight, 15-20 parts of rhizoma coptidis, 15-50 parts of radix scutellariae, 20-30 parts of lithospermum, 15-25 parts of safflower carthamus, 15-20 parts of myrrh, 15-50 parts of raw rhubarb, 50-100 parts of pseudo-ginseng, 15-50 parts of polygonum cuspidatum, 40-70 parts of zinc oxide, 0.8 part of anisodamine, 150 parts of borneol and 320-380 parts of sesame oil. The invention further discloses application of the topical drug composite in the preparation of drugs treating skin injury which comprises skin burn, skin scald, skin ambustion, skin lesions caused by radiation and chemotherapy, bedsore, and skin fester caused by other reasons.
CN102166194A Preparation method of anthocyanidin pellet The invention discloses a preparation method of anthocyanidin pellets. The method comprises the following steps of: grinding anthocyanidin and excipient till particle size is from 5 to 20 microns by fine-grinding technology, uniformly mixing, adding adhesive, and adopting pellet-forming technology to obtain anthocyanidin pellets, particle size being from 0.5 to 2.5 microns. The pellet comprises 10 to 80% by weight of anthocyanidin, 15 to 85% by weight of excipient and 2 to 8% by weight of adhesive. The method provided by the invention increases dissolution speed of the anthocyanidin, and improves bioavailability. Besides, the method is easy in operation, low in investment cost and easy to promote.
CN101156886A A composition for regulating intestinal canal flora and improving hypoxiatolerance force as well as its preparation method The invention relates to composition for adjusting intestinal flora and enhancing anoxia tolerance. The invention is characterized in that the composition is composed of the raw materials with the following parts by weight: 1 part of soy-bean oligosaccharide, 0.9 to 0.97 parts of spirulina powder, 0.3 to 0.4 parts of rhodiola root extractive, 0.15 to 0.25 parts of dextrin, and 0.02 to 0.04 parts of magnesium stearate. The invention has the advantages that the composition can adjust the intestinal flora and enhance the anoxia tolerance.
US20120029048 Phenylalkyl n-hydroxyureas for treating leukotriene related pathologies The method of treating patients by administering N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea for treatment of leukotriene related pathologies and compositions for this use.
EP2453891A1 Use of a melatonin agonist for the treatment of sleep disorders including primary insomnia Embodiments of the invention include the treatment of a sleep disorder comprising the administration of N-[[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4- yl)cycloproply]methyl]propanamide or a salt, stereoisomer, solvate, or hydrate thereof, in amorphous or crystalline form.
US20100183702 Therapies For Cancer Using RLIP76 The present invention is a composition identified as a region of ralA binding protein 1, wherein the region neighbors a membrane-associated portion of the ralA binding protein 1, reduces transport activity and membrane association of the ralA binding protein 1 and kills cells undergoing uncontrolled cell growth in a subject that has cells undergoing uncontrolled cell growth. The region is used to generate medicines that kill malignant cells and tumorigenic cells. Medicines may be in the form of antibodies, si-RNA and small molecules that recognize the region.
WO2004019959A3 Dna repair enzymes The invention relates to methods of selection of agents and compositions for the treatment of proliferative diseases such as cancer. More specifically, the present invention relates to the methods of selecting compounds which modulate the activity of DNA repair enzymes HAB1 and HAB2 and their uses in the treatment of disorders, which would benefit from an increase or a decrease in HAB1 or HAB2 activity.
CN101596204A Compound fluconazole ointment and preparation method thereof The invention relates to a compound fluconazole ointment prepared from fluconazole, neomycinsulphate, vaseline, lanolin, liquid paraffin, stearic acid, span-80, span-85, tween-80, sorbic acid, A-200, A-380, glycerol, DMF, ethyl acetate and distilled water. The invention uses new-generation triazole type medicine fluconazole to substitute nystatin in erfuling, combines fluconazole and neomycinsulphate to treat deep mycotic infection and has favorable curative effect. The ointment has enlarged antimicrobial spectrum, enhanced bacterium resistance and reduced toxic or side effect and can achieve the effect of deep therapy. Medicine-sensitive and clinical experiments indicate that the invention can effectively control the itch disease of the auditory canals of animals and the infection of mould fungi and microzyme in the skin and the auditory canals, is also effective to the local mycotic infection of dogs and cats and also can treat any possible primary and secondary bacterial infection. The compound fluconazole ointment is applied to the surfaces of the skin and the auditory canals and can effectively relieve inflammatory reactions and itch.
US20090022804 Chemoembolisation A composition for chemoembolotherapy of solid tumours comprises particles of a water-insoluble water-swellable synthetic anionic polymer and, absorbed therein an anthracycline. Suitably the polymer is a poly(vinyl alcohol) based polymer and the drug is doxorubicin.
EP1708706A1 Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and a dopamine agonist The invention relates to a pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety, or a tautomer, a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof (1), and at least one dopamine agonist or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof (2), and a pharmaceutically acceptable carrier or excipient, and optionally one or more other therapeutic ingredients.
CN103054810A High encapsulation rate curcumin albumin nano pharmaceutical composition The invention provides a pharmaceutical composition of curcumin and albumin nano particles, and a preparation method of the pharmaceutical composition. The albumin is made from human serum albumin or bovine serum albumin, or is prepared by taking ovalbumin as a raw material; and preferentially, the albumin is made from human serum albumin. The pharmaceutical composition prepared by the invention has better encapsulation rate.
CN1568966A Usage of baicalin and its derivatives, analogs in the preparation process of tumor resisting medicine The invention relates to baicalin and its derivatives, analogs, and the usage of baicalin and its derivatives, analogs in the preparation process of tumor resisting medicine.
CN101190221A Vitamin B6 chewable tablets for dog or cat The invention discloses a vitamin B6 chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the existing tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 5 to 20 percent of vitamin B6.
CN101390877A Preparation method of natural montmorillonite emergency haemostatic for external use Disclosed is a preparation method for an external natural bentonite emergency life-saving hemostatic agent, which adopts natural bentonite as raw material; the total content of silica and alumina is more than 70%; the interlayer spacing of natural bentonite is 1.0-2.0nm; the specific surface area of natural bentonite is 30-1000m2/g; the preparation include the steps: a herbal grinder is adopted to crush the massive natural bentonite into particles with different sizes; the particle sizes of the particles are 1micron-1mm; the crushed natural bentonite or ca-bentonite processed with ion-exchange is processed for 1-24 hours under the temperature of 60- 900 DEG C to obtain external natural bentonite emergency life-saving hemostatic agent which has the advantages of simple preparation operation, rich raw materials, cheap price, easy obtaining, convenient application and good hemostatic effect.
EP1906917A2 Oral, quickly disintegrating film, which cannot be spit out, for an antiemetic or antimigraine agent The invention relates to a film-shaped, single-layered and cavity-free preparation that does not contain any surfactants nor effervescent additives and flavor masking agents, comprised of film forming agents, one or more gelling agents and of one or more active substances selected from the group of antiemetics and antimigraine agents.
CN103083227A Ribavirin slow release nasal gel used for treating cold and preparation method of gel The invention belongs to the field of pharmacy, and relates to ribavirin slow release nasal gel used for treating cold and flu and a preparation method of the gel. The main components of the ribavirin slow release nasal gel comprise broad-spectrum and strong antiviral ribavirin in effective dose as a main drug and chitosan as the nasal gel matrix. The preparation method comprises the steps of: mixing the ribavirin with the chitosan to form sol gel; adding a preservative; then adjusting the pH value to 5.8-6.2 by using a pH adjusting agent; mixing uniformly; and sterilizing and packaging so as to finish the preparation. According to the invention, the water-soluble gel is adopted as a substrate to prepare the ribavirin nasal gel; the preparation process is simple; and the ribavirin slow release nasal gel remains in the nasal cavities for a long time and has a certain slow release effect, so that the biological utilization rate of the ribavirin slow release nasal gel is added, a good treatment function of the ribavirin slow release nasal gel is played, and low toxic and side effect is caused. The ribavirin slow release nasal gel used for treating cold has a relatively strong inhibition effect on the common infected influenza virus, and is convenient and comfortable to use.
EP2760861A1 Crystalline hydrochloride salt of (1- (4 -fluorophenyl) - 1h - indol - 5 - yl) - (3- (4- (thiazole - 2 - carbonyl) piperazin- 1 - yl) az etidin- 1 -yl) methanone and its use in the treatment of pain and metabolic disorders The present invention relates to a crystalline hydrochloride salt of (l-(4-fluorophenyl)-lH-indol-5-yl)(3-(4-(thiazole-2-carbonyl)piper- azin-l-yl)azetidin-l-yl)methanone, Formula (I) methods of making said salt, pharmaceutical compositions contain¬ ing said salt, and the use of said salt in the treatment of pain and dis¬ eases that cause such pain, and metabolic disorders such as, obesity, hyperphagia, and diabetes.
US20120245202 Methods and products for treating inflammation Pharmaceutical compositions comprising an isolated form of a compound of Formula I or IA (e.g., anatabine or S-(−)-anatabine) or a salt thereof can be used to treat disorders comprising an inflammatory component, including chronic, low-level inflammation. Compounds of Formula I also can be provided, for example, in other vehicles such as beverage products and consumer products such as lotions and creams.
WO2011046991A3 Certain substituted ureas as modulators of kinase activity At least one compound of Formula I or a pharmaceutically acceptable salt thereof, are provided herein. Pharmaceutical compositions comprising at least one one compound of Formula I or a pharmaceutically acceptable salt and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one compound of Formula I or a pharmaceutically acceptable salt effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one compound of Formula I or a pharmaceutically acceptable salt as a single active agent or administering such at least one compound of Formula I or a pharmaceutically acceptable salt in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one compound of Formula I or a pharmaceutically acceptable salt under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
US20080241101 Nutrient broth comprising serine protease inhibitors and cytokine for use propgation of skin basement membrane tissues; regenerative medicine; tissue repair The invention provides an epidermal basement membrane structure formation accelerating preparation and a skin external preparation comprising a serine protease inhibitor, and optionally an accelerator of production of extracellular matrix protein components of the epidermal basement membrane. It also provides, as a means for producing artificial skin having an adequately formed basement membrane, an artificial skin-forming medium which comprises a serine protease inhibitor, and optionally an accelerator of production of extracellular matrix protein components of the epidermal basement membrane and a matrix metalloprotease inhibitor, as well as a method for producing the same.
US20110319372 Method of diagnosing and therapeutically treating a patient for a traumatic brain injury Known or suspected traumatic brain injuries may be treated therapeutically by administering a therapeutically effective dose of resibufogenin. A preferred method for determining if a patient has a traumatic brain injury includes obtaining a body specimen from the patient, determining the concentration of marinobufagenin in the body specimen, comparing the concentration of marinobufagenin to the concentration in such body specimens in normal patients, and if the marinobufagenin concentration is substantially above the concentration of a normal patient, concluding traumatic brain injury exists. In a preferred embodiment, a substantial elevation is deemed to be an increase of about 30 percent above the marinobufagenin concentration of a normal patient. The body specimen may be blood, urine, or cerebrospinal fluid. If a substantial elevation is deemed to exist, the magnitude of the departure from the concentration of a normal patient may be employed in determining the timing and nature of treatment provided to the patient. The method may be repeated at predetermined intervals to monitor changes in the marinobufagenin with time.
WO2005063218A3 Pharmaceutical formulations of bisphosphonates A pharmaceutical formulation comprising an oral dosage form containing a bisphosphonic acid or a salt thereof and an inactive ingredient selected from: an ester of a medium chain fatty acid, or a lipophilic polyethylene glycol ester, said inactive ingredient having a hydrophilic lipophilic balance (HLB) of from about 1 to about 30.
CN102670498A Sustained-release sirolimus ophthalmic preparation The invention relates to a sustained-release sirolimus ophthalmic preparation for ophthalmic external use. The sustained-release sirolimus ophthalmic preparation is prepared by taking sirolimus as a pharmacodynamic raw material, taking bletilla striata polysaccharide gum as a sustained-release agent and adding appropriate auxiliary materials, wherein the using amount of the bletilla striata polysaccharide gum is equal to the ratio of the sirolimus to the bletilla striata polysaccharide gum of 1.0:(0.5-5.0). By taking the bletilla striata polysaccharide gum as a mucosal adhesive polymer medicine release system, the problem that the sirolimus is low in solubility and stability in a pure aqueous solution is solved; and by the effects of astringing, stopping bleeding, clearing heat, promoting diuresis, reducing tumescence and promoting tissue regeneration of bletilla striata, the immunosuppression effect and the ocular tissue penetrability of the sirolimus are improved.
WO2014122658A1 Amorphous calcium carbonate for accelerated bone growth The present invention provides a method for accelerating bone growth in a subject having a bone condition, selected from the group consisting of a fracture by external force, pathological fracture, fatigue fracture, distraction osteogenesis, osteotomy, osseointegration and combinations thereof, the method employing the administration of a composition containing stable amorphous calcium carbonate, comprising at least one stabilizer. Further provided are the orally-administrable pharmaceutical compositions for use in accelerating bone growth in said bone conditions.
WO2009144253A1 Compounds comprising a 3-pyridinol or 5-pyrimidinol ring having an organoseleno or organotelluro substituent for use as antioxidants Compounds comprising a 3-pyridinol or 5-pyrimidinol ring carrying an organoseleno- or organotelluro- substituent on the pyridine or pyrimidine ring, exhibit useful antioxidant properties. The compounds may for example be in accordance with the following formula (I) as defined herein. Catalytic chain-breaking and hydroperoxide decomposing antioxidant properties are also disclosed. Furthermore the compounds may be used in combination with a reducing agent. The compounds are useful for the stabilization of man-made and natural materials, or for the prevention or treatment of disorders caused by or involving free radical-mediated or oxidative tissue damage.
CN102746227A Dimemorfan phosphate crystal form II and preparation method thereof, and pharmaceutical composition The invention provides a method for preparing dimemorfan phosphate crystal form II, which comprises the following steps: adding a crude dimemorfan phosphate product into methanol, heating under reflux to dissolve the crude dimemorfan phosphate product, cooling to precipitate crystals, filtering, and drying to obtain the solid dimemorfan phosphate crystal form II. The dimemorfan phosphate crystal form has the following X-diffractometer diagram characteristics; and in the X-ray powder diffractogram, interplanar distance d and Bragg angle 2theta represent the relative intensity relative to the percentage of the strongest line. The invention also provides a pharmaceutical composition containing the dimemorfan phosphate crystal form II as an active component and one or more proper auxiliary materials, such as tablets, capsules, granules, oral liquids, syrups, suspensoids and injections. The dimemorfan phosphate crystal form II has favorable pharmaceutical values, and has the characteristics of favorable purity, definite crystal form, excellent reproducibility and the like; and the dimemorfan phosphate crystal form II has valuable physiological activities in the field of preparations, and can be stored for a long time while remaining high stability.
CN101897827A Method for controlling quality of red medicinal gel The invention discloses a method for controlling quality of red medicinal gel. In the method, the contents of pseudo-ginseng and diphenhydramine hydrochloride in the red medicinal gel are detected by adopting a high performance liquid chromatography method, and effective substances are identified. Requirement to the method is improved based on National Formulary and national standard, and the method represents the advantages of simple operation, detection conservation, reagent toxicity reduction, specificity improvement and the like.
WO2013192091A1 Compounds with (1e, 6e)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disstituted-hepa-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereof The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
WO2010033543A3 Substituted benzamides as cannabinoid receptor ligands Disclosed herein are cannabinoid receptor ligands of formula (I), wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
US20090202545 Melanoma biomarker and methods of uses The present invention relates to the use of TROY, also called tumor necrosis factor receptor superfamily, member 19 (TNFRSF 19) also called toxicity and JNK inducer (TAJ), in diagnosis and therapy of non-epithelial cancers, such as melanoma. Accordingly, the invention provides in vitro and in vivo diagnostic and/or prognostic methods for cancers, other than epithelial cancers, preferably melanoma, comprising analyzing TROY expression in a biological sample from an individual or in an individual, wherein expression of TROY in non-epithelial cells, such as in melanocytes, in indicative the biological sample or the individual containing malignant cells, such as malignant melanoma cells. The invention also provides therapeutic use of TROY targeting molecules, such as TROY antibodies or TROY targeting RNA interfering agents for treatment of cancer wherein the cancer cells express TROY.
US20120308644 Compositions for mucosal delivery of agents Compositions and methods for mucosal delivery of agents are provided. The compositions are intended for administration to mucosal surface, such as oral, gastrointestinal and nasal mucosa. The compositions provided contain one or more mucoadhesive proteins and an agent to be delivered. Methods for delivery of agents using the compositions provided herein are also provided.
US20080287407 Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
CN102453074A Pentacyclic triterpene saponin and application thereof The invention relates to the medical technical field, in particular to a pentacyclic triterpene compound which is separated to be obtained from a ranunculaceae plant of pulsatilla cernua (Thunb.) Bercht.et Opiz, and the chemical structural formula is shown in the accompanying drawing, wherein glc, rha and ara respectively represent beta-D-glucopyranose, alpha-L-pyrane rhamnose and alpha-L-pyrane arabinose, and the compounds A and B are respectively a new compound. Cell experiments in vitro show that the compound has a remarkable protection function to neuroblastoma cell strain SH-SY5Y induced by A beta (25-35). The compound disclosed by the invention has the advantages of simpleness in preparation and remarkable activity. The invention provides the new compound for preventing and curing AD (Alzheimer's Disease). In the invention, the glc, rha and ara respectively represent beta-D-glucopyranose, alpha-L-pyrane rhamnose and alpha-L-pyrane arabinose.
CN103275161A 3-hydroxyl cholest-6-keto aromatic aldehyde azine steroidal compound, synthetic method of steroidal compound and application of steroidal compound in preparation of anti-tumour drug The invention relates to a 3-hydroxyl cholest-6-keto aromatic aldehyde azine steroidal compound with an azine structure. The structural formula of the steroidal compound is described in the specification. Experiments prove that the 3-hydroxyl cholest-6-keto aromatic aldehyde azine steroidal compound has an obvious inhibiting effect on multiple tumour cell strains and can be applied to preparation of a drug used for treating cancer.
US7115649 Methods of treating skin disorders using thio-oxindole derivatives The present invention provides methods of treating skin disorders includes delivering to a mammal a composition containing a compound of formula I, or tautomers thereof, in a regimen, wherein formula I is: and wherein R1–R5 and Q1 are defined as described herein. Specifically, methods for treating acne, hirsutism, and a composition for conditioning the skin are described.
CN102349903A New pharmaceutical composition containing levoamlodipine and valsartan and preparation method thereof The invention relates to a new pharmaceutical composition containing levoamlodipine and valsartan and a preparation method thereof. The pharmaceutical composition is composed of amlodipine besilate, valsartan, microcrystalline cellulose, compressible starch, cross-linked sodium carboxymethylcellulose, silicon dioxide and magnesium stearate, wherein amlodipine besilate is levoamlodipine besylate crystal; and the composition is a completely new oral solid pharmaceutical composition. The powder of the pharmaceutical composition has better compressibility, fluidity, shaping property and lubrication property; and the adopted direct tabletting method has simple and reasonable process and good repeatability. The dissolubility of the pharmaceutical composition is more than 90% by adopting less disintegrant; and the pharmaceutical composition has the advantages of better stability and rapider disintegration. The composition contains a new levoamlodipine besylate crystal, and the crystal significantly improves the dissolubility of levoamlodipine besylate, thus the composition has better treatment effect.
CN101129506B Capsule pill drops for treating electro-optical eye and anti-inflammation detoxication Disclosed is a process for preparing capsules and pills for treating eye inflammation caused by electro-optical, wherein the which is prepared from glucose as the host, as well as goldthread root, mulberry leaf and honeysuckle flower. The medicament can be used for treating a plurality of eye diseases, or for protecting eyes, improving eyesight and eye fatigue. The invention realizes simple formulation, low cost of preparation. easy production, easiness in use, and precise curative effect.
WO2006030803A1 Purinenucleoside derivative modified in 8-position and medicinal use thereof A purinenucleoside derivative modified in the 8-position which is useful for diseases attributable to abnormality in plasma uric acid level. It is a purinenucleoside derivative modified in the 8-position which is represented by the following formula (I), a prodrug or pharmacologically acceptable salt of the derivative, or a hydrate or solvate of any of these. They are useful in the prevention or treatment of gout, hyperuricemia, urinary stones, hyperuric nephropathy, etc. In the formula (I), n is 1 or 2; RA is hydrogen or hydroxy; R1 is hydrogen, hydroxy, thiol, amino, or chlorine; and ring J is, e.g., optionally substituted 2-naphthyl or a group represented by the following general formula (II) (wherein Y is a single bond or connecting group; ring Z is optionally substituted aryl, heteroaryl, etc.; and R2 to R4, P1, and Q each is halogeno, cyano, etc.).
US8791120 Fast-dissociating dopamine 2 receptor antagonists The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
WO2008002816A1 Substituted benzamide modulators of the histamine h3 receptor Certain substituted benzamide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
DE102004059674A1 Transdermal delivery system to treat movement disease and post-operative illness comprises scopolamine and a matrix comprising styrene-butadiene-copolymer-bonding adhesive Transdermal delivery system (A) comprises scopolamine (I) as active substance and a matrix (II) comprising styrol-butadiene-copolymer-bo nding adhesive. - ACTIVITY : None given. - MECHANISM OF ACTION : None given.
CN1843494A Compound econazole nitrate zedoary turmeric oil emulsion type foam aerosol and its preparation method The invention relates to a compound aromatic turmeric oil emulsion type foam aerosol of Econazole nitrate and its preparing process, wherein each 1000mL of the aerosol contains the following constituents (by mass ratio): Econazole nitrate 1-100g, aromatic turmeric oil 1-200g, emulsifying agent 5-250g, preservative agent 0.1-20g, projection agent 50-500g, and balancing dissolvent. The aerosol can be used for treating vaginitis, cervical erosion and uterine neck disease.
CN101125145A Local using prostaglandin micro emulsion and its preparation method The present invention discloses a locally applied prostaglandin micro-emulsion and the preparation method thereof, the present invention is a liquid or semi-solid preparation which is composed of prostaglandin E1 or the derivatives and the pharmaceutical acceptable excipients, the present invention is characterized in that the present invention contains the prostaglandin E1 or the derivatives, oil phase, emulsifiers, assistant emulsifiers and water, which may also contain the osmotic promoting agents, thickeners and preparation stabilizers; the present invention is characterized by transparent or translucent solution, stable thermodynamics, simple preparation process and so on. The micro-emulsion prepared by the present invention has good transdermal permeability and provides a safe and effective new preparation for the clinical medication of the prostaglandin E1 or the derivatives. The present invention can treat the erectile dysfunction by urethral administration and can treat the ulcers on the four limbs caused by chronic arterial occlusive disease, the resting pains on the four limbs caused by microcirculation disorder and other diseases by external application.
CN103450042A Chlocibutamine compound and pharmacy-acceptable salts thereof The invention relates to a chlocibutanmine compound, a preparation method thereof, and an application of the compound in preparation of drugs for curing epilepsy.
WO2014011814A1 Tri-salt form of metformin Provided herein are tri-salt compounds comprising a compound having two acidic functional groups and one basic functional groups (e.g., aspartate or glutamate), metformin, and polyunsaturated fatty acids, such as eicosapentaenoate or docosahexaenoate. The salts can be used in the treatment of diabetes, diabetes with concomitant dyslipidemia (e.g. , high triglycerides) and diabetes exacerbated cardiovascular complications, such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke. The compounds of this invention are also useful in treating obesity.
US20120156301 Methods and Compositions for Treating and Preventing Symptoms of Hormonal Variations The present invention relates to methods, compositions, and kits for treating or preventing symptoms of hormonal variation. The method comprises the steps of administering an effective amount of Dextromethorphan or Dextrorphan, or a pharmaceutically acceptable salt thereof, to a subject having one or more symptoms of hormonal variations.
US20080227741 Zap-70 expression as a marker for chronic lymphocytic leukemia / small lymphocytic lymphoma (cll/sll) It has been surprisingly found that ZAP-70 expression, both at the protein and mRNA levels, is indicative of clinical subgroups of CLL/SLL patients. In particular, high ZAP-70 expression is indicative of Ig-unmutated CLL/SLL. Methods are provided for discriminating between clinical subgroups of CLL/SLL, by determining whether subjects overexpress ZAP-70 mRNA or protein.
CA2370697C Adjuvant composition comprising saponin and an immunostimulatory oligonucleotide The present invention relates to adjuvant compositions which are suitable to be used in vaccines. In particular, the adjuvant compositions of the present invention comprises a saponin and an immunostimulatory oligonucleotide, optionally with a carrier. Also provided by the present invention are vaccines comprising the adjuvants of the present invention and an antigen. Further provided are methods of manufacture of the adjuvants and vaccines of the present invention and their use as medicaments. Methods of treating an individual susceptible to or suffering from a disease by the administration of the vaccines of the present invention are also provided.
CN102976999A Acetic acid [2-(2,5-dioxo-2,5-dihydro-1-pyrryl) ethyl] ester compound and synthetic method thereof The invention discloses an acetic acid [2-(2,5-dioxo-2,5-dihydro-1-pyrryl) ethyl] ester compound and a synthetic method thereof. The acetic acid [2-(2,5-dioxo-2,5-dihydro-1-pyrryl) ethyl] ester compound is synthesized by using maleic anhydride, ethanolamine and glacial acetic acid as raw materials, adopting the glacial acetic acid as solvent and adopting one-pot reaction through acylation, closed-loop and esterification reactions. The synthetic method for the acetic acid [2-(2,5-dioxo-2,5-dihydro-1-pyrryl) ethyl] ester compound disclosed by the invention has the advantages that the raw materials are cheap and easy to obtain, the production cost is low, and the synthetic process is simple, green and environment-friendly; the product is easy to separate and high in purity; and the yield of the finish products is 30-35%.
CN103432506A Pharmaceutical composition for treating upper respiratory infection The invention relates to a pharmaceutical composition for treating upper respiratory infection. The pharmaceutical composition is a medicament which is prepared from the following raw material medicines: muskmelon seed, folium sennae, fructus perillae, black soya beans, ormosia, lophatherum gracile, elsholtzia, terminalia chebula retz, cockscomb, flos daturae, Chinese azalea flowers, Semen Cuscutae, Gorgon fruits, Amomum tsao-ko, roses, zaocys dhumnade, marmor serpentinatum, spina gleditsiae, piemarker, ovateleaf holly barks, Platycodon grandiflorum, Chinese violet, Chinese Starjasmine Stems, lignum pini nodi tumorisati, exocarpium benincasae, valeriana jatamansi jones, kamuning, indigoplant, cortex dictamni, teasel root, humifuse euphorbia herb, potentilla chinensis, pillis ophidiae, vine of multiflower knotweed, fructus polygoni orientalis, Sedum sarmentosum. Scorpio, honeysuckle stems, lindley eupatorium, swertia mileensis, madder, radix tinosporae, liquidambar formosana hance, agilawood, dayflowers, szechwan Chinaberry fruits, lotus stamen, longan aril, ternate buttercup root and folium Turpiniae. The pharmaceutical composition provided by the invention is reasonable in formula and exact in curative effect, and can be used for effectively treating upper respiratory infection.
DE102008009752A1 Beverage for improving the state of health, contains chili pepper juice and grape fruit juice that are mixed to the beverage without alcohol The beverage for improving the state of health, contains chili pepper juice and grape fruit juice that are mixed to the beverage without alcohol.
CN102895231A Cefuroxime and sulbactam pharmaceutical composition The present invention provides a cefuroxime and sulbactam pharmaceutical composition which is composed of cefuroxime or salt powder thereof and sulbactam or salt powder thereof, and contains cefuroxime or salt powder thereof with a particle size of 106-150 [mu]m. The pharmaceutical composition has good dissolubility and dissolution rate, effectively ensures the product quality, and has important significance for safety and efficacy of the pharmaceutical.
CN102091135A Bezoar antidotal pills (tables and capsules) containing bezoar cultured in vitro and preparation method thereof The invention provides bezoar antidotal pills (tables and capsules) containing bezoar cultured in vitro and a preparation method thereof. Based on weight part, the bezoar antidotal pills (tables and capsules) are prepared from 1 part of bezoar cultured in vitro, 10 parts of realgar, 40 parts of gypsum, 40 parts of rhubarb, 30 parts of baical skullcap root, 20 parts of platycodon root, 5 parts of borneol and 10 parts of liquoric root. Compared with the prior art, the preparation provided by the invention has fewer toxic and side effects and is exact in treatment effectiveness, and the preparation process is more reasonable.
WO2007011232A3 Lipid lowering agents for increasing bmd The invention comprises the use of a fibrate and/or the compound Wyeth 14,643 for preparation of a pharmaceutical composition for the prevention and/or treatment of conditions associated with low/decreased bone mineral density (BMD), and/or for increasing the BMD by decreasing the bone resorption.
US20110010784 Insulin-like gene of prawns and uses thereof Nucleic acid molecules encoding an insulin-like factor of the androgenic gland of the freshwater prawn Macrobrachium rosenbergii (M. rosenbergii) are disclosed. Also disclosed are methods of silencing the expression of the insulin-like factor gene in decapod crustaceans order, particularly in M. rosenbergii, useful for producing male monosex populations.
US20100120814 Crystalline and Amorphous Forms of Naltrexone Hydrochloride The present invention relates to novel crystalline forms of naltrexone hydrochloride including hydrated and solvated forms and a novel amorphous form. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline and amorphous forms of naltrexone hydrochloride, as well as methods of treating addictive behavior by administering the pharmaceutical compositions.
US20100292261 Quorum sensing antagonist, method of preventing a biofilm formation using the quorum sensing antagonist and method of reducing a bacterial contamination using the quorum sensing antagonist In the quorum sensing antagonist blocking the communication in bacteria, the method for preventing biofilm formation using this quorum sensing antagonist and the method for reducing the bacterial contamination, the quorum sensing antagonist contains the homoserine lactone moiety and sulfanylethanoyl group, and has a similar chemical structure to that of the autoinducer which is produced by bacteria as a signal, whereby the quorum sensing antagonist can inhibit the formation of biofilm and reduce the bacterial contamination as well.
CN101240006B Oleanane triterpene compound with C ring containing conjugated double bond and use thereof The invention provides a oleanane triterpenoid compound containing conjugate double bonds in C ring, having a general formula indicated in formula (1). The inventive compound has activity in inhibition of tumor cell growth, and can be applied in preparing medicament for treatment of tumor diseases. The inventive compound also has obvious inhibition of mouse ear edema caused by dimethylbenzene, and can be used in preparing anti-inflammatory medicament. General formula indicated by formula (1) is also disclosed.
CN101371925B Nano silver-cell growth factor sustained-release composite body as well as preparation method and use thereof The invention relates to a sustained-release matter of a cell peptide growth factor. The invention further relates to a preparation method of the sustained-release matter of the cell peptide growth factor and a use thereof. The provided sustained-release matter of the cell peptide growth factor is a nano-silver-cell growth factor complex, the peptide growth factor bonds with Ag by the nano-absorption or/and -COO, -CN and -H, thereby being absorbed on the surface of the nano-silver to form the complex. The sustained-release matter utilizes the natural anti-inflection effect of the nano-silver to provide a clean micro-environment for the biological action of the growth factor, promotes faster repair and healing of wound/wound surface, reduces adverse reactions, reduces the times of drug administration and the waste of drugs, alleviates suffering of patients and simultaneously reduces medical costs.
CN101829119A Cefodizime sodium composition and powder injection The invention relates to a cefodizime sodium composition, which comprises the following components in percentage by mass: 99.00 to 99.99 percent of cefodizime sodium crystals and 0.01 to 1.00 percent of sodium benzoate. The invention also relates to a preparation containing the cefodizime sodium crystals and the sodium benzoate and a method for preparing the cefodizime sodium crystals. The cefodizime sodium crystals have the advantages of high stability and good liquidity.
WO2014017046A1 Prophylactic and/or therapeutic agent for radiation damage The present invention addresses the problem of providing a prophylactic and/or therapeutic agent for radiation damage, which has a novel mechanism of action, can prevent and alleviate a wide variety of conditions of radiation damage for which there has been no therapeutic means previously, and is highly safe for human bodies. A prophylactic and/or therapeutic agent for radiation damage, which contains a compound represented by formula (I) (wherein R1 represents a hydrogen atom or an acyl group; and R2 represents a hydrogen atom, a linear or branched alkyl group, a cycloalkyl group, an aryl group or an aralkyl group) such as 5-aminolevulinic acid (5-ALA) or a salt thereof as an active ingredient, can be used for improving survival rates, improving the decrease in body weights, or alleviating hematopoietic injury.
CN1934945A Use of imazalil for sunitary product and sterilizer product and its use method The present invention discloses the application of imazalil in sanitary articles and disinfectant products and its application method. Said product imazolil can be made into sanitary article for curing beri-beri, can be used as disinfectant for sanitary equipment, can be made into disinfectant for cleaning pudendum of human body and can be used as detergent for washing clothes. Its application method includes the following steps: making imazolil into sulfate, making the imazolil surfate and water into its solution preparation, said imazolil surfate solution can be directly used or diluted firstly and then can be used.
US20130236570 Use of hypertonic saline to draw fluid out of swollen tissue and relieve nasal congestion The optimum concentration of salt in solutions to combat congestion of the mucosa is a relatively narrow range. This use of in hypertonic saline solutions for treatment of congestion of the mucosa having a concentration within the range of 2.3% to 2.7% w/v sodium chloride/water with the most preferred concentration being 2.4% to 2.6% w/v of sodium chloride in water brings maximum relief of congestion without causing irritation or discomfort.
US20090227562 Combination of a Selective Noradrenaline Reuptake Unhibitor and a PDEV Inhibitor The present invention relates to a combination of a selective noradrenaline reuptake inhibitor (NRI) and a phospho-diesterase type 5 (PDEV) inhibitor. Such a combination is particularly useful in the treatment of pain.
US20130029939 Novel glucokinase activators and methods of using same Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure wherein R1, R2, R3, R4, R5, R6, Y and X are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related disease employing the above compounds is also provided.
WO2011089289A1 Use of amitriptyline as antitumour agent for the treatment of lung cancer Pharmaceutical composition comprising the tricyclic antidepressant amitriptyline for the preparation of a medicament for the treatment and/or prophylaxis of a cancerous lung process. Preferably said cancerous lung process is non-microcytic and, more preferably, the cancerous non-microcytic lung process is large-cell lung carcinoma.
CA2369413C Transmembrane protein expressed in prostate and other cancers A prostate tumor associated gene (designated 24P4C12) and its encoded protein is described. 24P4C12 is highly expressed in prostate tissue xenografts, providing evidence that it is turned on in at least some prostate cancers. 24P4C12 provides a diagnostic and/or therapeutic target for prostate and other cancers.
WO2010023161A1 Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
CN101723939A Isopentenyl-oxyl substituted dehydrogenized silybin ether and preparation method and application thereof The invention relates to Isopentenyl-oxyl substituted dehydrogenized silybin ether and the preparation method and the application thereof. The compound has the activity of eliminating extracorporeal extracorporeal 1-diphenyl-2-picrylhydrazyl radical, the activity of obviously inhibiting the generation of lipid peroxide induced by radical and the function of powerfully preventing the damage of therat adrenal pheochromocytoma PC12 cells due to the hydrogen peroxide, i.e. the function of preventing the oxidative damage of the PC12 cells simulating the brain nerve cells, thereby playing a positive role in preventing the brain cell tissue oxidation and brain never oxidation and preventing and treating the senile dementia and other neurodegenerative diseases. The pharmacodynamic result shows that 7-site substituted dehydrogenized silybin ether can be expectantly used for preparing the medicament for preventing and treating the neurodegenerative diseases.
CN101548966A Application of salvianolic acid A in salvia miltiorrhiza The invention discloses a new application of salvianolic acid A in salvia miltiorrhiza, particularly an application of salvianolic acid A in salvia miltiorrhiza in the preparation of a medicament for curing cerebrovascular endothelial dysfunction. The content of the salvianolic acid A in salvia miltiorrhiza is equal to or higher than 50 percent and lower than 100 percent, and preferentially, the content of the salvianolic acid A in salvia miltiorrhiza is equal to or higher than 90 percent and lower than 100 percent. The pharmacodynamics mechanism studies show that the salvianolic acid A in salvia miltiorrhiza has good protection action to the cerebrovascular endothelial dysfunction.
US7687620 [1,4]diazepino[6,7,1-IJ]quinoline derivatives as antipsychotic and antiobesity agents Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided: where R1 through R7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
CN103393709A Pharmaceutical use of cytosine arabinoside prodrug The invention belongs to the field of medicines, and provides a use of a cytosine arabinoside prodrug for preparing medicines for treating female patients with liver cancer but not suitable for men or excluded from use by men. Untoward effects generated by delivery of the cytosine arabinoside prodrug can be reduced or even avoided. In addition, the invention further provides a pharmaceutical preparation with high content of the cytosine arabinoside prodrug, so that the lifetime of critical patients with liver cancer can be prolonged, wherein the pH system can further increase the stability of the cytosine arabinoside prodrug.
CN1857228A Oral gatifloxacin disintegrant and its preparing process The present invention provides an oral gatifloxacin disintegrant and its preparation process. The oral gatifloxacin disintegrant contains gatifloxacin in 20-75 wt% and medicinal supplementary material in 25-80 wt%, and the medicinal supplementary material includes one or several of disintegrating agent, stuffing, wetting adhesive, lubricant and coating material. The preparation process of the oral gatifloxacin disintegrant includes coating medicine powder or medicine carrying micro pill and tabletting. The oral gatifloxacin disintegrant of the present invention has the advantages of fast medicine release, increased absorbing points and less local excitation on gastrointestinal tract and is suitable for taking without using water and by patient with dysphagia.
US20110311474 Novel Tricyclic Compounds The invention provides compounds of Formula (I) and Formula (II) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
US7084176 N-arylphenylacetamide derivatives and medicinal compositions containing the same N-Arylphenylacetamide derivatives represented by the following formula [I]: (wherein R1 is C1-6 alkoxy, etc.; R2 is hydrogen, —(CH2)m—N(R6)(R7) (m is an integer of from 1 to 4; R6 is hydrogen, C1-4 alkyl, etc., R7 is hydrogen, etc.), etc.; R3 is hydrogen, halogen, etc.; R4 is C6-10 alkyl, —Y—R8 (Y is a single bond, C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, etc., R8 is aryl, C3-8 cycloalkyl, C6-15 polycycloalkyl, etc.), etc.; R5 is hydrogen, etc.; and X1 is hydrogen), or pharmaceutically acceptable salts thereof or hydrates or solvates of the same, and a pharmaceutical composition containing the same. These compounds are useful as preventives and/or remedies giving no pain at the early stage of administration, which are efficacious in oral administration and have potent analgesic and antiinflammatory effects.
US20080107637 Using inhalabe gas comprising ethyl nitrite as means of nitrosylating hemoglobin, delaying tumor growth and preventing destruuctive tissue damage associated with inflammation The presently disclosed subject matter provides methods for increasing perfusion in hypoxic regions of tissues in subjects. Also provided are methods for treating diseases and/or disorders associated with hypoxia in subjects, methods for increasing sensitivity of tumors to radiation and/or chemotherapy treatments, methods for delaying tumor growth in subjects, and methods for inhibiting tumor blood vessel growth in subjects. In some embodiments, the presently disclosed methods involve administering to subjects in need thereof a first composition selected from the group consisting of a nitrosylated hemoglobin and an agent that induces nitrosylation of endogenous hemoglobin in the subject and a second composition comprising a hyperoxic gas. In some embodiments, the presently disclosed methods also include treating a tumor with radiation therapy, chemotherapy, photodynamic therapy, immunotherapy, or combinations thereof. Also provided are inhalable gases that can be employed in the presently disclosed methods.
US20110265786 Inhalable Formulations For Treating Pulmonary Hypertension And Methods Of Using Same The present invention is directed to an inhalable formulation for the treatment of pulmonary hypertension in a mammal (e.g., humans), wherein the formulation comprises at least one hypertension reducing agent, including but not limited to an angiotensin converting enzyme inhibitor, angiotensin receptor blocker, beta-blocker, calcium-channel blocker or vasodilator, or any combination thereof. The formulations of the present invention may be a solution or suspension, and preferably are suitable for administration via nebulization. The present invention is also directed to a method and kit for treating a mammal suffering from pulmonary hypertension.
CN101715453A heterocyclic compounds and their uses Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity. The present invention also enables methods for treating cancers that are mediated, dependent on, or associated with p110 activity, including but not restricted to leukemias, such as acute myeloid leukaemia (AML), myelo-dysplastic syndrome (MDS), myelo-proliferative diseases (MPD), chronic myeloid leukemia (CML), T-cell acute lymphoblastic leukaemia (T-ALL), B-cell acute lymphoblastic leukaemia (B-ALL), non Hodgkins lymphoma (NHL), B-cell lymphoma and solid tumors, such as breast cancer.
EP1578722A2 Kinase inhibitor scaffolds and methods for their preparation General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
EP1781304B1 Use of organic glucosamine salts The present invention relates to the use of an organic glucosamine salt selected from glucosamine glucuronate, glucosamine ascorbate, glucosamine malate, glucosamine hydrogen malate, glucosamine citrate, glucosamine hydrogen citrate, and glucosamine dihydrogen citrate for the preparation of a medicament for the treatment of arthrosis and inflammation and pain associated with arthrosis. The present invention also relates to the use of an organic glucosamine salt, selected from the ones mentioned above, for the preparation of a nutritional supplement acting as a chondroprotector, to nourish the cartilage, protect the joints, prevent water deficit in the tissues that form the joint, improve the joints' functional capacity, elasticity, and flexibility, and prevent and revert the physical overexertion syndrome in athletes, and the effects associated therewith.
US20120108550 Use of Derivatives of Polyunsaturated Fatty Acids as Medicaments Use of polyunsaturated fatty acid derivatives as medicaments or functional foods. The present invention relates to the use of 1,2-fatty acid derivatives in the treatment or prevention of common diseases whose etiology is based on alterations (of any type) of the cell membrane lipids, for example, changes in levels, in the composition or in the structure of these lipids. In addition, for diseases in which the regulation of lipid composition and of the structure of the membranes (or proteins that interact with membranes) causes the reversion of pathological state.
CA2223407C Oxidant scavengers The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating intra- and extracellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.
CN101613345B Preparation method of silibinin ether substituted by diolefin propyl and medical application thereof The invention relates to a preparation method of silibinin ether substituted by diolefin propyl and a medical application thereof, in particular to the preparation of a silibinin ether derivative substituted by A and E ring diolefin propyl and a medical application thereof in preparing a medicine for preventing and treating cerebral nerve cellular oxidation injury and senile dementia caused by oxygen free radicals. A pharmacological experiment validates that the compound has a very strong resisting function to PC12 cell injury caused by free radicals, namely, an obvious antioxidation injury protection function to PC12 cells simulating cerebral nerve cells, and can be anticipatively developed into a medicine for protecting the cerebral nerve cells, resisting oxidation and preventing and treating senile dementia.
CN1947716A Clathrate compound of alpha-lipoic acid-cyclodextrin derivatives, and its prepn. method An inclusion compound of alpha-thioctacid and cyclodextrin derivative with high water solubility and stability and no odor is prepared from alpha-thioctacid and cyclodextrin derivative in weight ratio of 1: (0.5-2000). Its preparing process is also disclosed.
US20110178110 Genotype and Expression Analysis for Use in Predicting Outcome and Therapy Selection The invention provides compositions and methods for determining the likelihood of successful treatment with a various treatment regimens available to gastrointestinal cancer patients. After determining if a patient is likely to be successfully treated, the invention also provides methods for treating these patients.
WO2014088657A1 C20'-urea derivatives of vinca alkaloids A vinca alkaloid compound that is substituted at the 20'-position with a urea or thiourea group is disclosed. The urea's proximal nitrogen atom bonded to the 20'-position carbon atom is secondary, whereas the distal nitrogen atom can be unsubstituted only when the compound contains an optionally present 10'-fluoro substituent, and is otherwise preferably mono- or di-substituted. Methods of preparing the compounds are disclosed as are compositions for their use and methods of treatment using a compound.
CN103432107A Tapentadol hydrochloride paracetamol orally disintegrating tablet and preparation method thereof The invention provides a tapentadol hydrochloride paracetamol orally disintegrating tablet and a preparation method thereof. According to the invention, the content of tapentadol hydrochloride is 37.5 mg-75.0 mg (by tapentadol), and the content of paracetamol is 325 mg; taste masking coating is conducted on the tapentadol hydrochloride and the paracetamol respectively to allow the tablet to be suitable for oral taking; selecting and using pharmaceutic adjuvant suitable for physicochemical properties of the tapentadol hydrochloride and the paracetamol to conduct coating; finally blending uniformly and tabletting. The fluidity of raw materials used for the prescription and the taste masking coating is good to facilitate the tabletting; the taste of the medicine is masked after being subjected to coating, and meanwhile, a corrigent is added to conduct taste adjustment for oral use. Therefore, a suitable disintegrating agent is selected and used to allow the orally disintegrating tablet to be able to achieve the requirement of quick disintegration.
CN1839834A Eye medicine for preventing and treating asthenopia and allergy Disclosed is a compound preparation for treating and preventing eye strain and allergy, which comprises (by weight percent) taurine 0.1-99.9%, naphazoline hydrochloride 0.01-99.9%, vitamin B6 0.01-99.9%, chlorpheniramine maleate 0.01-99.9%, and right amount of auxiliary therapeutic medicaments such as menthol, sodium hyaluronate, glycerine and medicinal findings such as preservative agent and buffering agent.
CN101380303A Anti-cancer medicine sustained-released injection loaded with platinum compound and synergist thereof A anticarcinogenic slow release injection carrying platinum compounds and a synergist thereof is composed of slow release microspheres and a dissolvant, wherein, the slow release microspheres comprise anticancer active components and a slow release adjuvant, and the dissolvant is a special dissolvant containing a suspending agent. The anticancer active component comprises platinum compounds such as sunpla, dicycloplatin, eptaplatin, (cis-amminedichloro(2-methylpyridine) platinum, camphoramine chloroacetic platinum or picoplatin, and the like, and a cytotoxic drug selected from a phosphoinositide 3-kinase inhibitor, pyrimidine analogue and/or a DNA repair enzyme inhibitor; the slow release adjuvant is biocompatible macromolecules such as polylactic acid and copolymer thereof, polyethylene glycol, carboxyl end polylactic acid copolymer, copolymer of dienoic fatty acid and sebacic acid, poly (erucic acid dimer-sebacic acid), poly (fumaric acid-sebacic acid), polifeprosan, polylactic acid, EVAc, and the like, and the suspending agent has the viscosity of 100cp-3,000cp (at the temperature of 20-30 DEG C) and is selected from sodium carboxymethyl cellulose, and the like. The slow release microspheres can also be made into a slow release implant. The slow release injection is injected or placed in tumors or around the tumors, which can improve the curative effects of non-operative therapies such as radiotherapy, chemotherapy, and the like.
WO2007126001A1 Antitussive or expectorant pharmaceutical composition comprising loxoprofen An antitussive or expectorant pharmaceutical composition comprising loxoprofen and one or more members selected from caffeine, ephedrine and codeine.
US20080027083 Modulators of chemokine receptor activity crystalline forms and process The present invention provides a novel antagonist or partial agonists/antagonists of MCP-1 receptor activity: N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein. Compounds that are useful intermediates of the process are also provided herein.
EP2133089A1 Compositions for the treatment of disorders of the upper respiratory tract and influenza syndromes The present invention relates to compositions based on benzophenanthridine alkaloids, extract of Hippophae rhamnoides and extract of Echinacea angustifolia which possess antibacterial, antiviral and antiinflammatory activity, and are useful in the treatment of bacterial and viral infections of the upper respiratory tract, and in the treatment of influenza.
US20090117167 Injectable capsaicin with vasocontrictor adjunctive agent Disclosed in certain embodiments is a method for relieving pain at a site in a human or animal in need thereof, comprising administering by injection or infiltration, a dose of a capsaicinoid and coadministering a vasoconstrictor.
CN102114067A Compound oviductus ranae granules and application thereof The invention provides compound oviductus ranae granules and an application thereof, and the compound oviductus ranae granules contain the following raw materials: oviductus ranae, acanthopanacis senticosi polysaccharides, ginsenoside, red bilberry anthocyanins, chlorogenic acid, vitamin C and vitamin E. The compound oviductus ranae granules have good oxidation resistance, radiation resistance, anti-overweight property, anti-low pressure property, anti-fatigue property and good effect of improving organism immunity. The compound oviductus ranae granules can improve the athletic ability of an animal from the overall level and improve the spatial discrimination type learning and memorization ability; the observation of cell ultra-structure proves that the compound oviductus ranae granules have obvious effect of protecting hippocampal neuronal mitochondria and hepatic and splenic cell mitochondria from being injured; and the molecular level proves that the compound oviductus ranae granules have the effects of affecting gene expression, regulating an immune factor and improving immunity. The compound oviductus ranae granules further have the effects of improving the total anti-oxidation ability, improving the ability of inhibiting hydroxy radicals, reducing triglyceride and low density lipoprotein-cholesterol (LDL-C) in serum, improving high density lipoprotein-cholesterol (HDL-C) in the serum, and reducing weight.
DE102009026357A1 Mixed oxide dispersion in water, where mixed oxide contains silicon, sodium, and either potassium, calcium, phosphorus and/or magnesium, useful to manufacture or prepare a food-, pharmaceutical- or cosmetic product Mixed oxide dispersion in water, is claimed, where the mixed oxide contains silicon, sodium, and either potassium, calcium, phosphorus and/or magnesium. Independent claims are included for: (1) the preparation of the mixed oxide dispersion, comprising mixing silicon dioxide, sodium compound, either calcium-, phosphorus-, magnesium- and/or calcium compound and/or optionally alumina and/or either a chromium-, cobalt-, iron-, copper-, manganese, molybdenum-, selenium-, vanadium-, zinc- and/or tin compound, cooling the obtained mixed oxide composition, pulverizing the mixed oxide composition and dispersing the milled mixed oxide composition; (2) a food composition, pharmaceutical composition or cosmetic product comprising the mixed oxide dispersion; and (3) the preparation of a food composition, a pharmaceutical composition or a cosmetic product comprising preparing a preparation of the herbal raw material and mixing with the mixed oxide dispersion. - ACTIVITY : Anorectic; Antialcoholic; Dermatological. - MECHANISM OF ACTION : None given.
CN103224499A Pheophorbide curcumin ester with photosensitive activity and preparation method and application thereof The present invention discloses pheophorbide curcumin ester with photosensitive activity and preparation method and application thereof. The structure of pheophorbide curcumin ester with photosensitive activity is shown in formular I; the preparation method comprises mixing the pheophorbide acid and the curcumin at molar ratio of (1-5) :1 to be dissolved in the organic solvent, adding the catalyst under the protection of nitrogen for esterification reaction at the temperature of between 30 and 60 DEG C for 4 to 8 hours; rinsing the resultant reaction mixture with the saturated brine to obtain the organic phase to be dried, filtered and distilled at reduced pressure to obtain the pheophorbide curcumin ester with photosensitive activity; the dosage of catalyst accounts for 5 to 25% of that of raw materials, pheophorbide acid and curcumin; the organic solvent is one or more than one of chloroform, benzene and ethyl acetate. The pheophorbide curcumin ester provided by the present invention has characteristics of good targeting, long photosensitive wavelength, deeply tissue penetrating power and anti-tumor activity, and can be used as a novel photosensitizer applied to the photodynamic therapy.
CN102718726A (z)-5-benzylidene thiazoline-4-thiazoline derivative as immunomodulator The invention discloses a compound of general formula (I) or its pharmaceutically acceptable salts, wherein R1 and R2 are identical or different, R1 and R2 are respectively selected from hydrogen, halogen, nitro,-NRaRb,-SO2Rc,-SO2NRdRe,-CONRfGg,-NRhCORi,-NRjSO2Rk,azido, cyan-, trifluoromethyl, trifluoromethoxy, C1-C6 alkyl or C1-C6 alkoxy, and HO-C1-C5-O-(CH2)m-; R3 is selected from hydrogen, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, and halogen; R4 is selected from NR5R6 and -OCR7R8-CR9R10-(CR11R12)n-O-R13; or R3 and R4 are combined together to form methylenedioxy and ethylenedioxy capable of being optionally substituted by hydroxymethyl; R5 and R6 are independently selected from C1-C6 alkyl; R7 is selected from hydrogen, hydroxyl, and C1-C6alkyl or hydroxymethyl; R8, R9, R11 and R12 are independently selected from hydroxyl or methyl; n is a natural number selected from 1-5, and when n is 1, R10 is selected from hydroxyl, C1-C6 alkoxy, amino, and -NHR5 or -NR5R6, otherwise, R10 is selected from hydrogen and C1-C6 alkyl; m is a natural number selected from 1-8; R13 is hydrogen, C1-C6 alkyl, and halogen, 1-glyceryl or 2-glyceryl; and Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, Ri, Rj and Rk are independently selected from hydrogen, and C1-C6 alkyl or C6-C14 aryl.
WO2010129273A2 Butaclamol for the treatment of amyotrophic lateral sclerosis The present invention relates to the use of butaclamol and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases.
CA2272291C Crf antagonistic quino- and quinazolines This invention concerns compounds of formula (I), including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono-or di(C3-6cycloalkyl)methyl, C3 6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C1-6alkyl or C1-6alkyloxyC1-6alkyl; and Ar1 and Ar2 are each optionally substituted phenyl; and Het1 is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
CN103126979A Luteolin solution composition The invention relates to the medicinal cosmetic field and especially relates to a stable luteolin solution composition. The luteolin solution composition contains luteolin, alkaline amino acids and a solvent, wherein the weight ratio of luteolin to the alkaline amino acids is 1:0.1-1:4, and the solvent is propylene glycol or a propylene glycol and ethanol mixture. The luteolin solution composition can be used for preparing injections, medicines for controlling skin diseases, and cosmetics.
WO2007018320A1 Agent for prevention of graft loss, and screening method for the agent Disclosed is an agent for prevention of graft loss comprising an NKT cell ligand such as α-galactosylceramide. The agent can prevent the graft loss in clinical islet transplantation or the like, and therefore can contribute to the improvement in transplantation efficiency. Also disclosed is a method for screening a compound for use in the prevention/treatment of graft loss, which comprises selecting a compound capable of inhibiting the activation of an NKT cell, the production of IFN-Ϝ in a CD11b+ cell or the like. By using the method, it becomes possible to produce an agent for preventing/treating premature graft loss by a novel mechanism.
EP2275410A1 Process for production of compound having antagonistic activity on npyy5 receptor, and useful crystal Disclosed are process for producing a compound having NPYY5 receptor antagonism and useful crystals. A process for producing a compound represented by the formula (IV): wherein R1 is substituted or unsubstituted alkyl, R2 is substituted or unsubstituted alkyl, and n is 1 or 2, or the like, which comprises reacting a compound represented by the formula (II): wherein R1 and n are as defined, above, and X is a leaving group, or the like and a compound represented by formula (III): wherein R2 is as defined above, or the like.
EP1772462A2 Steroid sulfamates, method for the production and use thereof Gonadal and D-homo gonadal steroid derivatives of formula (I) and their salts are new. A double bond may be present between atoms 9 and 11, 8 and 9, 8 and 14, 14 and 15, 6 and 7 or 7 and 8; between atoms 8 and 9 and 14 and 15 or between 8 and 9 and 7 and 6, two double bonds may be present; or a cyclopropane or epoxide group with alpha or beta orientation may be present between atoms 14 and 15; atoms 2, 3, 4, 6, 7, 11, 12, 15, 16 and/or 17 are optionally substituted by 1-6C alkoxy, (1-4C alkoxy)(1-4C alkoxy), hydroxy(1-4C alkoxy), 1-6C alkanoyloxy or tris(1-4C alkyl)silyloxy or OH and in the case of the presence of a second OH group, a group such as ketal, thioketal, cyanohydrin, cyanosilylether or geminal hydroxyethynyl group may be present as a protecting group; n = 1 or 2; R1 = H, alpha - or beta -Me or beta -Et; R3 = H, halo (e.g. Cl, Br, I, At, F, 18F, and preferably additional residues R4 and/or R5 are present on atoms 1, 2, 3, 4, 6, 7, 11, 15, 16 and/or 17; R4 = aryl or 1-12C alkyl; R2 = H, 1-5C alkyl, 1-3C alkyl with an annelatted saturated ring, or aryl(1-3C alkyl); R6 = halo (e.g. Cl, Br, 76Br, F, 18F or At); and m = 1-5 (preferably 1-3); with the proviso that R3 is not H when m = 1 and the sulphamoyloxy group is attached to the aromatic A-ring.
CN1778312A High-exudation anabiotic liquid, its preparation and use thereof A high-osmosis analeptic liquid for treating the traumatic hemorrhagic shock and improving the average arterious pressure, central venous pressure, cardiac rhythm, heart output and system blood vessel resistance is proportionally prepared from sodium chloride, dextran and the water for injection through two-stage deluting.
CN103070849A Application of oxyresveratrol in preparing ovary aging resistant medicine The invention discloses an application of oxyresveratrol in preparing an ovary aging resistant medicine. The oxyresveratrol has significant treatment effects on various ovary aging diseases such as polycystic ovarian syndrome, dysfunctional uterine bleeding, premature ovarian failure and climacteric syndrome. The oxyresveratrol is prepared into the oral, transdermal or injection medicine for treating the ovary aging diseases.
CN101348504A Ruthenium mixed-polypyridyl complex, preparation thereof and use as antitumor drug The invention discloses a ruthenium polypyridyl complex and a method for preparing the same and an application thereof in antineoplastic medicines. The ruthenium polypyridyl complex is a ruthenium(II) complex which respectively takes 3'-deoxyadenosine or 2'-deoxyadenosine as a main ligand and bipyridyl(bpy), dimethyl bipyridyl(dmbpy) and phenanthrolines(phen) as auxiliary ligands. In the invention, firstly ruthenium trichloride, poly-pyridine and lithium chloride are dissolved in DMF and subjected to heating reflux under the argon shield for 8h to prepare crystals, and the crystals and deoxyadenosine are dissolved in absolute ethyl alcohol and subjected to reflux under the argon shield and at a temperature of 90 DEG C for 5h, and the solid coarse product is obtained through a column chromatography purification reaction, and the ruthenium polypyridyl complex is obtained. The ruthenium polypyridyl complex of the invention can be used as a chemotherapeutic drug to treat tumors.
CN102388047A Novel salts of sitagliptin The present invention relates to novel pharmaceutically acceptable salts of sitagliptin, to processes for their preparation and to pharmaceutical compositions containing them.
CA2585983C Use of 1,4-bis (3-aminoalkyl) piperazine derivatives in the treatment of neurodegenerative diseases Use of 1,4-bis (3-aminoalkyl) piperazine derivatives as defined in formula I or II for the manufacture of a pharmaceutical composition intended for the treatment of neurodegenerative diseases, related neurodegenerative diseases, developmental diseases or cancer. The instant invention is also directed to some specific 1,4-bis (3-aminoalkyl) piperazine derivatives and pharmaceutical composition including them.
CN101392007B Anti-tumor manganese complexes using mitochondria as target point and preparation and use thereof The invention relates to a micromolecule compound having the functions of anti-tumor and autophagy, a preparation method and the application thereof. The micromolecule compound is a manganese complex L<1>MnCl2 and L<2>MnCl, wherein, the L<1> represents ethyl 2-dipyridyl methylamino propanoate; and the L<2> represents 2-dipyridyl methylamino propanoic acid. The manganese complex is obtained through chemosynthesis by taking the ligand L<1> or L<2> and the MnCl2 as main materials. The manganese complex of the dipyridyl methylamine ligand provided by the invention has strong inhibition effects on the growth of tumor cells A549, Hela, HepG-2 and Eca109, can inhibit the swelling of the mitochondrial induced by the calcium ion and induce the apoptosis of the tumor cells by means of autophagy; the micromolecule compound can be used as new anti-tumor activity medicine which takes the mitochondria as target spot and as the tumor cell autophagy agent for applying to the drug tolerance tumor therapy.
US20050026867 Hyaluronic acid-associated superoxide dismutase mimics and their use in the treatment of joint pain Herein is disclosed a composition, comprising a superoxide dismutase mimic (SODm) associated with hyaluronic acid (HA), wherein the composition is a liquid at about 37° C. The composition is useful in a method of treating pain or inflammation in a joint of a mammal, comprising (i) providing the composition and (ii) injecting the composition into or close to the joint.
US20120115905 Nitrone, Nitroso, and Nitroxide Spintraps and Spin Labels and Their Hydroxylamines Nitrone, nitroso, and nitroxide spintraps and spin labels and their reduction products are claimed for the prevention and treatment of fibrocystic disease of breast, premenstrual dysphoric syndrome and associated symptomology, prevention and treatment of migraine headache, cyclic vomiting syndrome, rectal hemorrhoids, trigeminal neuralgia, peripheral vascular disease, influenza, peridontitis and gingivitis, herpes zoster, herpes simplex, and post-herpetic neuralgia.
CN103181920A Anti-cancer vegetable oil recipe The invention provides an anti-cancer vegetable oil recipe, and relates to vegetable oil recipes. The recipe includes: 5000-5550 mg of glutamic acid, 3000-3280 mg of aspartic acid, 3000-3160 mg of arginine, 1000-1610 mg of phenylalanine, 1000-1500 mg of glycine, 1000-1320 mg of tyrosine, 1000-1250 mg of proline, 1000-1050 mg of valine, 1000-1030 mg of alanine, and 800-930 mg of lysine. The anti-cancer vegetable oil recipe has extraordinary role on the body's growth and development, body immune, cardiovascular healthcare and other aspects, and has the efficacy of anti-cancer, protecting liver, protecting myocardial health, enhancing immunity, anti-aging and the like.
US7534805 Imidazole derivatives, their preparation and their use as medicaments Novel imidazole compounds of the formula wherein the substituents are as defined in the application having antitumoral activity and use thereof.
EP2050452A1 indenoisoquinolines as topoisomerase inhibitors I useful as antineoplastic agents A number of indenoisoquinolines were prepared and evaluated for cytotoxicity in human cancer cell cultures and for activity vs. topoisomerase I. The two most cytotoxic indenoisoquinolines proved to be cis-6-ethyl-5,6,12,13-tetrahydro-2,3-dimethoxy-8,9-(methylenedioxy)-5,11-dioxo-11H-indeno[1,2-c]isoquinoline and cis-6-allyl-5,6,12,13-tetrahydro-2,3-dimethoxy-8,9-(methylenedioxy)-5,11-dioxo-(11H)indeno[1,2-c]isoquinoline. Two of the most potent topoisomerase I inhibitors were 6-(3-carboxy-1-propyl)-5,6-dihydro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline (26) and 6-ethyl-2,3-dimethoxy-8,9-(methylenedioxy)11H-indeno[1,2-c]isoquinolinium chloride (27). Two additional potent topoisomerase I inhibitors, 6-allyl-5,6-dihydro-2,3-dimethoxy-8,9-(methylenedioxy)-5,11-dioxo-11H-indeno[1,2-c]isoquinoline (13c) and 5,6-dihydro-6-(4-hydroxybut-1-yl)-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-(11H)indeno[1,2-c]isoquinoline (19a), did not unwind DNA and did not affect topoisomerase II.
US20110301109 Phenylpyrimidone Compounds, the Pharmaceutical Compositions, Preparation Methods and Uses Thereof The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.
EP1237886B1 Meglumine salt of a specific quinolinecarboxylic acid compound active on nmda receptors The present invention relates to a novel salt of enantiomer A of 7-chloro-4-(2-oxo-1-phenyl-3-pyrrolidinylidene)-1,2,3,4-tetrahydro-2-quinoline carboxylic acid or a solvate thereof, to processes for its preparation, to pharmaceutical compositions containing it and to its use in therapy and in particularly its use as medicine for antagonising the effects of excitatory amino acids upon the NMDA receptor complex.
WO2009086934A1 Composition for treating scalp and skin The invention relates to a composition containing in a soluble form and in an aqueous phase: - proteins: 0.40% to 0.45%; - calcium: 0.50% to 0.51%; -the following mineral salts: sodium, potassium, magnesium, phosphorus, sulphur; - the following trace elements: selenium, manganese, iron, zinc, copper; - acetic acid: 4.70%. The invention also relates to a method for obtaining the composition that comprises placing raw poultry eggs with their shells in a tank containing diluted acetic acid and sodium chloride for one month so that the composition contains the solubilised forms of the compounds naturally occurring in the shell of a poultry egg. The composition of the invention can be used for preparing a drug or a cosmetic product for treating skin or scalp alopecia.
WO2012117969A1 Anti-inflammatory agent and process of producing same Provided is a material which is safe and inexpensive, can be ingested easily and continuously on a daily basis, and has a significant anti-inflammatory activity. An anti-inflammatory agent comprising a mixture of: a soybean seed or an extract thereof each of which has been activated by a light irradiation treatment and/or a heating treatment; and chlorophyll.
CN102579537A Medicament for treating diabetic foot and deep ulcer The invention relates to a medicament for treating diabetic foot and deep ulcer. A conventional treatment method of the diabetic foot has certain curative effect at the moment, but causes long-term unhealing of foot ulcer due to foot paralysis, thus having poor effect. The medicament is prepared in the following steps: crushing naphthalene, borneol, pseudo-ginseng, musk and zinc oxide into fine powder in a proportion, and mixing. According to the medicament, harmful bacteria in deep focus can be killed in a short time, so that the root that various stubborn ulcers are hard to completely heal can be solved. The medicament is a medicament for treating diabetic food and deep ulcer with simple drugs, low cost and good curative effect.
WO2011162733A1 Antibacterial and/or antifungal component having the property of binding specifically to bacteria and/or fungi The invention relates to pharmacology, veterinary medicine, cosmetology, medicine, and the food and preserving industries. Moreover, the claimed product can be used as a disinfectant and a hygiene product. What is proposed is: an antibacterial and/or antifungal component having the property of binding specifically to bacteria and/or fungi. Said component comprises antibacterial and/or antifungal viruses which have been altered such that the replication function of said viruses is disrupted. The claimed component makes it possible to quickly transform the production of medicinal and veterinary preparations, cosmetics, preservatives, hygiene products and disinfectants to target newly appearing strains of microorganisms.
CN102176909A 2-hydroxy-ethanesulfonate salt The invention provides (R) -1- [3- (R) -cyclohexyl-hydroxy-phenyl- methyl) -isoxazol-5-ylmethyl] -3- (3-f luoro-phenoxy) -1-azonia- bicyclo[2.2.2]octane 2-hydroxy ethanesulf onate, pharmaceutical compositions containing the compound and its use as a muscarinic antagonists, for the treatment of chronic obstructive pulmonary disease.
US20050142100 Tumor Necrosis Factor Binding Protein (TBP) or an isoform, mutein, fused protein, function derivative, active fraction, or salt; multiple sclerosis; corticosteroid; glatiramer The invention relates to the use of an agent having, stimulating or maintaining tumor necrosis factor (TNF) activity, together with an interferon (IFN) for treating and/or preventing demyelinating diseases, in particular multiple sclerosis (MS). The use of a combination of a TNF or a tumor necrosis factor binding protein in combination with an interferon for treating and/or preventing demyelinating diseases is preferred.
CN1995065B Fusion protein for suppressing PTTG expression and its coding gene and uses The invention discloses a fusing protein and coded gene and application to inhibit PTTG in the positive PTTG tumour drug, which makes 1-30th amino acid residue on the PBF of connecting peptide connect beta-TrCP 1-256th amino acid residue on the N end.
WO2011094290A1 Pyrazolopyrimidine kinase inhibitors The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
US20110105621 Method of reducing brain cell damage, inflammation or death A method of reducing the occurrence of brain cell damage or death caused by transient cerebral hypoxia, ischemia, brain inflammation or a traumatic brain injury (TBI) event. The method typically comprises identifying a subject with transient cerebral hypoxia, ischemia, brain inflammation or a TBI, and within 24 hours of onset of the condition, administering to the subject a continuous intravenous infusion dose of methamphetamine in an amount sufficient to reduce the occurrence of brain cell damage or death caused by the condition. Preferably, the dose is increased in response to a delay in administration. The invention also relates to a method for modulating cytokine expression within the brain to treat such conditions.
US20070238708 Acute Inflammatory Condition Treatment This invention provides a method for prophylaxis or treatment of an acute inflammatory disorder, comprising administering to a patient an effective amount of pharmaceutically acceptable bodies carrying an effective number of phosphate-containing groups presented or presentable on the surface of said bodies, the phosphate-containing groups comprising a plurality of phosphate-glycerol groups or groups convertible to such groups, to inhibit and/or reduce the progression of the acute inflammatory disorder, said bodies being of a size from about 20 nanometers (nm) to 500 micrometers (μm).
CN103690532A Effect of atorvastatin on preparation of drug for treating pulmonary hypertension The invention relates to a new use of a drug, and specifically relates to an effect of atorvastatin on preparation of a drug for treating pulmonary hypertension. The invention discovers for the first time that atorvastatin is capable of alleviating MCT (Monocrotaline)-induced pulmonary inflammation, and inhibiting pulmonary vascular remodeling, pulmonary artery rising and right ventricular hypertrophy without affecting the body circulating pressure; NF-kB is possible to play an important role in the MCT-induced pulmonary hypertension; the atorvastatin is capable of inhibiting the inflammatory reaction by reducing the expression of the MCT-induced pulmonary hypertension lung tissue NF-kB, and is capable of reducing pulmonary vascular remodeling and inhibiting the pulmonary artery high pressure rising; therefore, the atorvastatin can be applied to preparation of the drug for treating the pulmonary hypertension.
WO2007016757A1 Stabilized extended release pharmeceutical compositions comprising an hmg-coa reductase inhibitor The present invention is a new stable extended release drug composition particularly suitable for use as an antihypercholesterolaemic or antihyperlipidaemic agent. The present invention is specifically a drug composition comprising a pharmaceutical, a complexing agent and a matrix-forming agent, and a method for manufacturing same. When applied to acid-labile drugs like HMG-CoA reductase inhibitors, the resulting drug composition is stabilized and is characterized by an extended-release profile.
CA2133144C Vitamin d3-analogs The invention relates to the compounds 1,25-dihydroxy-16-ene-24-oxo-cholecalciferol and 1,24,25-trihydroxy-16-ene-cholecalciferol which stimulate differentiation of HL-60 cells, rendering them useful as an agent for the treatment of neoplastic diseases such as leukemia, and also decrease proliferation of human keratinocytes, rendering them useful as an agent for the treatment of hyperproliferative disorders of the skin such as psoriasis. They are prepared by perfusing 1,25-dihydroxy-16-ene-cholecalciferol in rate kidneys, extracting the perfusate and isolating 1,25-dihydroxy-16-ene-24-oxo-cholecalciferol and 1,24,25-trihydroxy-16-ene-cholecalciferol.
US20100111990 Polypeptide Recognized by Anti HIV-1 GP41 Antibodies Isolated from Highly HIV-1 Exposed, Non Infected Women The invention relates to a polypeptide recognized by anti HIV-1 gp41 antibodies isolated from Highly Exposed, non Infected Women, and epitopic fragments and conjugate thereof. Method of inducing antibodies neutralizing HIV-1 against HIV-1 is also contemplated.
CN102871964A Stable and efficient propofol middle/long-chain fat emulsion injection and preparation method thereof The invention relates to a stable and efficient propofol middle/long-chain fat emulsion injection and a preparation method thereof. The injection consists of propofol, soybean oil, middle-chain triglyceride fatty acid, lecithin, oleic acid, glycerol, a pH regulator and water for injection, and is characterized in that the weight contents of soybean oil and middle-chain triglyceride fatty acid are not equal, and especially, the content of soybean oil is higher than that of middle-chain triglyceride fatty acid. The propofol middle/long-chain fat emulsion injection prepared according to the invention has the advantages of high stability and strong anesthetic effect.
US20100034768 Composition and method for treatment of insect bites A composition for treating wounds of the skin, such as those caused by the bites of small insects or jellyfish, includes a wax or resin, an emulsifier, and ammonium hydroxide. The composition is applied to the skin in a thin layer, and when it dries, it forms a thin, protective film over the wound. Application of the composition has been found to provide temporary and immediate relief of pain and/or itching. The protective film shields the wound, and therefore aids in healing. The composition can be made of any of a variety of waxes or resins, and the emulsion can be formed with long-chain alcohol or fatty acid soaps, such as oleic acid or triethanolamine.
US8236807 Quinoxalinyl macrocyclic hepatitis C serine protease inhibitors The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
CN1951391A Method for preparing suspension of rhodiola root nanoliposome The invention relates to a method for preparing gadol glycosides nanometer liposome suspension. Wherein, said suspension comprises the extractive of gadol as gadol glycosides and the nanometer liposome packing the gadol glycosides. The inventive production comprises that: dissolving the lecithin and cholesterol into absolute ether, depressurizing and vaporizing the organic solvent; adding gadol glycosides phosphate buffer with some surface activator, expanding, and dispersing at ultrasonic wave, to obtain the final suspension. The average grainness of product is lower than 100nm; the package rate of gadol glycosides can reach 25-35%.
WO2010068383A1 Novel rifamycin 3, 4- (3' -substituted aminomethyl) fused pyrrolo derivatives The present invention is directed to novel 3,4-(3'-substituted aminomethyl) fused pyrrolo rifamyacin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.
WO2009041565A1 Quinazolinone derivative, and prophylactic or therapeutic agent for corneal/conjunctival disorder comprising quinazolinone derivative as active ingredient A compound represented by the general formula (I) or a salt thereof exhibits excellent prophylactic and ameliorating effect on an age-related corneal disorder or the like in a pharmacological test using SAMP10, and is therefore useful as a prophylactic or therapeutic agent for a corneal/conjunctival disorder such as dry eye, superficial punctate keratitis and corneal epithelial defect. In the general formula (I), A1-A2 represents a group 1; X represents a group 2 or the like; Y represents a carbon atom or a nitrogen atom; a dashed line represents a single bond or a double bond; L represents a single bond, an alkylene group, a cycloalkenylene group or the like; R1a and R1b independently represent a hydrogen atom, a halogen atom or the like; R2 represents a hydrogen atom or a halogen atom; and R3 represents a hydrogen atom or a halogen atom.
CN103316034A Active attapulgite medicine and preparation method for same The invention relates to an active attapulgite medicine and a preparation method for the same. The active attapulgite is prepared by activating attapulgite powder with 325-400 meshes for 3-5 hours in a condition of 150-260 DEG C, and 20-100% in percentage by weight within the medicine; and the ratio of the diffraction peak height of christobalite in the active attapulgite to the characteristic peak height of attapulgite is less than 50.0%. The preparation method comprises the following steps of: pre-treating attapulgite clay to obtain an attapulgite crude material liquid, and ultrasonically dispersing to obtain a suspended emulsion; and separating the suspended emulsion to remove materials having a relative density of greater than 2.3 g/cm<3>, centrifugally separating, drying, crushing until the average grain diameter is not greater than 45 microns, and activating the prepared attapulgite powder at a high temperature, thus obtaining the active attapulgite powder. The active attapulgite powder is prepared into a powder without adding pharmaceutic adjuvants, or prepared into a powder, chewable tablets, dispersible tablets, and granules with adding a conventional amount of pharmaceutic adjuvants. The content of christobalite in the active attapulgite powder disclosed by the invention meets the national medicine standards; and christobalite is good in adsorbability and wide in application range.
CN101138544B Diclofenac or the salt partial film forming gel composition and uses thereof The present invention discloses a compound of an diclofenac or the halo-diclofenac local membrane forming gel, which comprises the components of the following weight percentages comprising 0.5 percentage to 7 percentage of alkyl cellulose, 1 percentage to 10 percentage of etherifying agent , 0.5 percentage to 5 percentage of cross linking agent, 75 percentage to 90 percentage of dissolvent, 0.1percentage to 3 percentage of diclofenac or the halo-diclofenac. The cross linking agent is the saturated fat or the alcoholic acid, the chemical general formula of which is CnH2n+2-m-l(OH)m(COOH)l. Among the formula, m or n or 1 is the integer and the n is no less than m, which is no less than 2. 1 is no less than 0 and the result of m plus 1 is 4 to 8. The result of n plus 1 is 4 to 8. In the present invention, the compound of the diclofenac or the halo-diclofenac local membrane forming gel is applied for relieving the local pain and inflammation of the organism tissue. A water drain protective membrane with smooth property, firm property, wear-resisting property and duration property is formed on the surface of the ulcer when the present invention is applied. Compared with all kinds of formulations of the diclofenac or the halo-diclofenac in the present technique, the membrane formed by the gel compound is not likely to experience fracture, dissolution or corrosion. The membrane has properties of long maintenance time and slow releasing of the medicine.
CN102247511A High-efficiency burn treating medicine and preparation method thereof The invention relates to a high-efficiency burn treating medicine and a preparation method thereof. The high-efficiency burn treating medicine comprises 3 to 7 parts of tea oil, 7 to 15 parts of aloe skin and other components. The preparation method comprises: extracting emodin from aloe by hot ethanol; and fully utilizing recovered aloe skin to prepare the high-efficiency burn treating medicine.The high-efficiency burn treating medicine also comprises 4 to 12 parts of mung bean and 2 to 5 parts of borneol, can effectively treat medium/light burn, has high inflammation diminishing capacity, and can clear heat, detoxify, moisturize skin, promote heal of wound surface and prevent scar after heal.
CN102397547A Anti-cancer pharmaceutical composition The invention relates to an anti-cancer pharmaceutical composition comprising arctigenin and a tyrosine kinase inhibitor. Compared to single-component medicines, the pharmaceutical composition provided by the invention has synergic anti-cancer activity in the aspect of non-small-cell lung carcinoma inhibiting. The invention also provides a micro emulsion preparation of the pharmaceutical composition.
US20090048200 GPR 26 G-Protein Coupled Receptor We disclose GPR26 G-protein coupled receptor (GPCR) polypeptides comprising the amino acid sequence shown in SEQ ID NO. 3 or SEQ ID NO: 5, and homologues, variants and derivatives thereof. Nucleic acids capable of encoding GPR26 polypeptide are also disclosed. The GPR26 receptor is useful in the diagnosis and therapy of mental illness.
WO2014139476A1 Epitope of rsv fusion protein and antibody identifying same Provided are an epitope peptide which can be used in the prevention of respiratory syncytial virus infections, or variants thereof and a recombinant protein comprising the epitope peptide or variants thereof with a carrier protein, and uses thereof. Also provided in the present invention are an antibody against these epitope peptides and cell strains generating the antibody, and uses thereof. Furthermore, also provided in the present invention are a vaccine comprising the recombinant protein or a pharmaceutical composition comprising the antibody, and the vaccine or pharmaceutical composition can be used for preventing symptoms related to respiratory syncytial virus infections.
US20090036413 Compositions, uses, and method of making wound care products from naturally occurring food ingredients Rationally designed wound care products made entirely of naturally occurring food ingredients that can be standardized and made available for the mass market using good manufacturing practice (GMP) guidelines, optionally, a safe food additive can be added. These products: are safe and effective; have an osmotic pressure compatible with optimal healing; are buffered to maintain optimal pH throughout the healing process; provide a protective barrier from further irritation and insult; control bacteria, viruses and fungi found in the skin and mucosa; nourish wounds; control excessive prolonged inflammation and thereby minimize scarring; minimize allergenic and irritation potential; are easy to use or apply; pass the preservative challenge test required for products intended for multiple use; contain fragrant essential oils to take advantage of the benefits provided by aromatherapy; can be individually optimized based on the diet of an individual or group of people.
US20120093916 Devices, Systems and Methods for Improving Memory and/or Cognitive Function Through Brain Delivery of SIRNA The present invention relates to devices, systems, and methods for improving memory and/or cognitive function by brain delivery of compositions of small interfering RNA or vectors containing the DNA encoding for small interfering RNA. Such compositions can be administered using devices, systems and methods for direct delivery of the compositions to the brain, or using devices, systems, methods of delivery, and compositions that deliver small interfering RNA or vectors containing the DNA encoding the small interfering RNA across the blood-brain barrier. The present invention also provides valuable small interfering RNA vectors, and methods for reduction of BACE1 levels in the hippocampus, cerebral cortex, or other regions of the brain that have beneficial effects on improving memory and/or cognitive function in a subject.
DE102005020331A1 New 5-substituted quinoline and isoquinoline derivatives are glucocorticoid receptor binders useful for treating inflammatory diseases e.g. alveolitis, Sjogren's syndrome, atopic dermatitis, acute lymphatic leukemia, rhinitis and emesis 5-Substituted quinoline and isoquinoline derivatives (A) and their racemates, individual stereoisomers, enantiomers, salts and prodrugs are new. 5-Substituted quinoline and isoquinoline derivatives (A) of formula (IIa) or (IIb) and their racemates, individual stereoisomers, enantiomers, salts and prodrugs are new. R1>, R2>H, 1-3C alkyl, halo, CN, 1-3C alkoxy or OH. An independent claim is also included for the preparation of (A). [Image] - ACTIVITY : Antiinflammatory; Respiratory-Gen.; Antirheumatic; Immunosuppressive; Antiallergic; Vasotropic, Dermatological; Antipsoriatic; Antipruritic; Nephrotropic; Hepatotropic; Gastrointestinal-Gen.; Ophthalmological; Auditory; Neuroprotective; Antibacterial; Cytostatic; Endocrine-Gen.; Antithyroid; Analgesic; Antidiabetic; CNS-Gen.; Cardiovascular-Gen.; Antiemetic; Hemostatic. - MECHANISM OF ACTION : Glucocorticoid receptor binder; Steroid hormone receptor binder; Androgen receptor binder; Mineralocorticoid receptor binder; Progesterone receptor binder; Cytokine secretion inhibitor. The ability of (A) to inhibit lipopolysaccharide induced cytokine interleukin-8 secretion was tested in human monocyte cell line THP-1. The results showed that the median inhibitory concentration of 5-[4-(5-fluoro-2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methylI-2-trif luoromethylpentylamino]-2-methylquinoline (II') was 5.9 nM.
CA2427560C Alkynyl amides and their therapeutic applications Compounds of formula (I), are novel and useful for treating seizure, migraine and psychiatric disorders.
US20110110986 High-yield activation of polymer surfaces for covalent attachment of molecules Polymer surfaces coated with organometallic layers, wherein the organometallic layers and polymer surfaces have functional groups that react to bond the organometallic layer to the polymer surface with organometallic functional groups remaining unreacted for the subsequent covalent attachment of organic overlayers. Coating methods and coated articles are also disclosed.
EP2464667A2 N-acylated octasaccharides activating fgfs receptors, their synthesis and their therapeutical application The invention relates to FGF receptor-activating N-acyl octasaccharides having Formula (I), wherein: R1 is an O-alkyl group optionally replaced by one or more aryl or cycloalkyl groups, R2 is an OSO3- or hydroxyl group, R3 is an alkyl, cycloalkyl, or alky-cycloalkyl group, R4 is a disaccharide having Formula (II), R6 is a disaccharide having Formula (III), and R8 is a disaccharide having Formula (IV), where R5, R7, and R9 have OSO3 or hydroxyl groups. The invention further relates to the preparation of said octasaccharides and to the therapeutic use thereof.
US20100197797 Methods of managing fibromyalgia using milnacipran The present invention relates to compositions comprising milnacipran or a pharmaceutically acceptable salt thereof (e.g., milnacipran hydrochloride) and methods for managing fibromyalgia comprising administering milnacipran or a pharmaceutically acceptable salt thereof (e.g., milnacipran hydrochloride). The present invention also relates to titration packs comprising dosage forms (e.g., tablets) comprising milnacipran or a pharmaceutically acceptable salt thereof (e.g., milnacipran hydrochloride) for oral administration. The titration packs enable patient compliance with a regime of changing dosage of the milnacipran or pharmaceutically acceptable salt thereof (e.g., milnacipran hydrochloride).
US8415480 Thiazolidine carboxamide derivatives as modulators of the prostaglandin F receptor The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery.
US20110201664 Methods and Compositions for Treatment of Prostate Intraepithelial Neoplasia Provided herein are methods of treatment of prostate intraepithelial neoplasia (PIN) by administering bexarotene. Also provided are pharmaceutical compositions and dosing regimens.
CN102008443A 4-amino-2-trifluoromethyl-phenylretinate solid dispersion and preparation method thereof The invention relates to the field of pharmaceutical compositions, in particular to a 4-amino-2-trifluoromethyl-phenylretinate solid dispersion and a preparation method thereof. The 4-amino-2-trifluoromethyl-phenylretinate solid dispersion is prepared by taking poloxamer 188 as a carrier, thus the dissolution speed and solubility of the solid dispersion are significantly improved. When the ratio of a drug to the carrier is more than 1:8, the accumulated dissolution rate of the solid dispersion within 60 minutes is over 95 percent. The solid dispersion and method provided by the invention have the advantages that because the solid dispersion is prepared by using a method combining a molten solvent and a filler, the drying step is accelerated, the brittleness of the obtained product is enhanced, and the obtained product is easy to crush; and meanwhile, the flowability of powder is increased, thereby overcoming the defects that the product prepared by the traditional drying method is large in viscosity, difficult to crush and poor in flowability, and facilitating the completion of subsequent preparation processes. The solid dispersion provided by the invention can be used for preparing antineoplastic drugs for inducing the differentiation of tumors.
EP1594574A2 Nk1 receptor antagonists for the treatment of functional dyspepsia The present invention relates to the use of NK1 receptor antagonists for the treatment of functional dyspepsia.
CN103450159A Piperidine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms, wherein, each group is described in the specification. The invention also relates to a preparation of the compound and a composition containing the compound, and the application of the medicine thereof.
CN101721568A Pharmaceutical composition for treating rheumatic arthralgia and preparation method thereof The invention discloses a pharmaceutical composition for treating rheumatic arthralgia and a preparation method thereof. The pharmaceutical composition adopts garden balsam stem, common monkshood mother root and garter snake for dispelling pathogenic wind, removing dampness, warming channels, dispelling cold and relieving pain; adopts cuttlebone and leech for invigorating pulse, removing stasis, activating collaterals and dredging meridian passage; and adopts clematis root, obscured homalomena rhizome and natural copper for strengthening tendons and bones, removing dampness, dredging channels and relieving pain, thereby having the effects of dispelling pathogenic wind, removing dampness, warming channels, dispelling cold, promoting blood circulation, removing blood stasis, strengthening tendons and bones, dredging channels, relieving pain and the like for treating arthritis, cervical spondylosis, intervertebral disc herniation, neuropathic pain, bone hyperplasia and the like.
EP2080779A1 Polymeric derivative of nucleic acid metabolic antagonist [PROBLEMS] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose. [MEANS FOR SOLVING PROBLEMS] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.
US20080280813 Complex drug delivery composition and method for treating cancer The present invention relates to compositions and methods for producing a complex drug delivery system which specifically targets cancer cells, has an increase in cellular uptake, is cytotoxic, and suppresses antiapoptotic cellular defenses.
CN102370710A Medicament for treating otitis media and preparation method thereof The invention relates to a medicament for treating otitis media and a preparation method thereof. The medicament for treating otitis media comprises the following major raw materials by weight: 6-60 grams of honeysuckle flower, 6-60 grams of weeping forsythia, 6-55 grams of red-rooted salvia root, 0.2-10 grams of dried alum, 0.2-10 grams of borneol and 0.5-10 grams of boric acid. The preparation method of the medicament for treating otitis media comprises the following steps of: distilling the honeysuckle flower and the weeping forsythia twice with a steam distillation method, and collecting a distillate; putting the distillate into a distillation device for redistilling, and collecting a re-distillate; decocting a mother solution together with decoction dregs and the red-rooted salvia root in two times, filtering with gauze to obtain a filtrate, and concentrating the filtrate to obtain a concentrated solution; adding an ethanol precipitate into the concentrated solution for removing impurities to obtain an alcohol-free concentrated solution, and concentrating the alcohol-free concentrated solution to obtain a re-concentrated solution; combining the re-concentrated solution with the re-distillate, and sterilizing for 40 minutes to obtain a combined solution; and adding a medicinal liquid of dried alum, borneol and boric acid into the combined solution, and adjusting the medicinal liquid with 95 percent ethanol till the alcohol content is 65 percent and the pH value of the solution is 7.5 to obtain the medicament.
WO2008021518A2 Crystalline forms of tiagabine hydrochloride and processes for the preparation of amorphous tiagabine hydrochloride The present invention provides 16 new crystalline forms of tiagabine hydrochloride.
US20080269149 Adeno-associated virus (AAV); genetic engineering; parvoviruses; gene therapy; muscle delivery; glioblastoma; Parkinson's Disease The present invention is based, in part, on the discovery that parvovirus (including AAV) capsids can be engineered to incorporate small, selective regions from other parvoviruses that confer desirable properties. The inventors have discovered that in some cases as little as a single amino acid insertion or substitution from a first parvovirus (e.g., an AAV) into the capsid structure of another parvovirus (e.g., an AAV) to create a chimeric parvovirus is sufficient to confer one or more of the desirable properties of the first parvovirus to the resulting chimeric parvovirus and/or to confer a property that is not exhibited by the first parvovirus or is present to a lesser extent.
WO2014056070A1 (-)-deprenyl and related compounds for the treatment of alopecia The present invention includes methods of preventing or minimizing cancer therapy induced alopecia (hair loss) in a subject, the method including administering to the subject an effective amount of (-)-deprenyl, a related compound, or a salt thereof. The present invention also includes methods of preventing or minimizing additional side effects of cancer therapies other than cancer therapy induced alopecia by the administration of an effective amount of (-)- deprenyl, a related compound, or a salt thereof.
US20120003158 Biomarkers for Inflammatory Bowel Disease and Methods Using the Same The present invention provides various biomarkers of inflammatory bowel disease, including biomarkers for Crohn's disease and biomarkers for Ulcerative colitis. The present invention also provides various methods of using the biomarkers, including methods for diagnosis of inflammatory bowel disease, methods for distinguishing between inflammatory bowel diseases, methods of determining predisposition to inflammatory bowel disease, methods of monitoring progression/regression of inflammatory bowel disease, methods of assessing efficacy of compositions for treating inflammatory bowel disease, methods of screening compositions for activity in modulating biomarkers of inflammatory bowel disease, methods of treating inflammatory bowel disease, as well as other methods based on biomarkers of inflammatory bowel disease.
WO2013170191A1 Methods of using antagonists of nad biosynthesis from nicotinamide Provided herein are NAD biosynthesis from nicotinamide antagonists (e.g., Nampt antagonists and/or NMNAT antagonists) and methods of using the same.
US7135493 HDAC inhibitor A compound having the following formula (I): wherein R1 is N-containing heterocyclic ring optionally substituted with one or more suitable substituent(s), R2 is hydroxyamino, R3 is hydrogen or a suitable substituent, L1 is —(CH2)n— (wherein n is an integer of 0 to 6) optionally substituted with one or more suitable substituent(s), wherein one or more methylene(s) may be replaced with suitable heteroatom(s), and L2 is lower alkenylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.
US20100272834 Freeze-Dried Molded Article Containing Magnesium Ascorbyl Phosphate The invention relates to freeze-dried molded articles containing magnesium ascorbyl phosphate and alginate as well as optionally one or more active substances and/or auxiliary substances. Furthermore, the invention relates to methods for manufacturing these freeze-dried molded articles, the combination of such freeze-dried molded articles in kit-of-parts arrangements together with aqueous solutions, as well as the use of the freeze-dried molded articles and the kit-of-parts combinations for pharmaceutical and cosmetic application.
EP1747785A1 Cyclodextrins for blood detoxification The present invention relates to the use of cyclodextrins for the preparation of a medicament for the prevention of septic syndrome and a method for removing bacterial endotoxins (lipopolysaccharides) from blood.
US20110230392 Novel narc sc1, narc 10a, narc 1, narc 12, narc 13, narc17, narc 25, narc 3, narc 4, narc 7, narc 8, narc 11, narc 14a, narc 15, narc 16, narc 19, narc 20, narc 26, narc 27, narc 28, narc 30, narc 5, narc 6, narc 9, narc 10c, narc 8b, narc 9, narc2a, narc 16b, narc 1c, narc 1a, and narc 25 molecules and uses therefor The invention provides isolated nucleic acids molecules and proteins, designated NARC SC1, NARC 10A, NARC 1, NARC 12, NARC 13, NARC17, NARC 25, NARC 3, NARC 4, NARC 7, NARC 8, NARC 11, NARC 14A, NARC 15, NARC 16, NARC 19, NARC 20, NARC 26, NARC 27, NARC 28, NARC 30, NARC 5, NARC 6, NARC 9, NARC 10C, NARC 8B, NARC 9, NARC2A, NARC 16B, NARC 1C, NARC 1A, and NARC 25, nucleic acid molecules and proteins. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing said nucleic acid molecules, host cells into which the expression vectors have been introduced, nonhuman transgenic animals in which a said genes have been introduced or disrupted, fusion proteins, antigenic peptides and antibodies to said proteins. Diagnostic and therapeutic methods utilizing compositions of the invention are also provided.
US20120258956 Use of a spirolide, analogues and derivatives for treating and/or preventing pathological conditions linked to the tau and beta-amyloid proteins The present invention is in the field of biomedicine. Specifically, it relates to the use of a spirolide compound with the chemical structure: for preparing a drug for the prevention and/or treatment of a pathology related to the increase in β-amyloid protein and/or hyperphosphorylation of tau protein compared to control, where said spirolide compound is administered in the amount necessary to reach a concentration in the serum of equal to or less than 50 nM. The amount administered is preferably the amount necessary to reach a concentration in the serum of between 0.5 nM and 50 nM.
CN101069709A Nutrient health-care capsule The present invention relates to a nutrient health-care capsule. Said nutrient health-care capsule is made up by using nutrient health-care active component xanthophylls, pearl powder, taurine and cyaniding through a certain preparation process. Said nutrient health-care capsule has several health0care functions of preventing angiocardiopathy and cerebrovascular disease and raising immunity of human body, etc.
US7544812 For example, 2-(4-{2-[1-(4-tert-Butyl-benzyl)-3-methyl-2-oxo-imidazolidin-4-yl]-ethoxy}-2-methyl-phenoxy)-2-methyl-propionic acid, 2-(4-{3-[1-(4-tert-Butyl-benzyl)-3-methyl-2-oxo-imidazolidin-4-yl]-propyl}-2-methyl-phenoky)-2-methyl-propionic acid; for treating diabetes mellitus The present invention is directed to compounds represented by the following structural Formula (I), (a) R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and —CH2—C(O)—R17-R18, wherein R17 is O or NH and R18 is optionally substituted benzyl; (b) R2 is selected from the group consisting of C1-C6 alkyl, C1-C6 alkenyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C1-C4 alkyl sulfonamide, C1-C4 alkyl amide, OR10 and C3-C6 cycloalkyl; (c) W is O or S; (d) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may optionally be replaced with O, NH, S, and optionally two carbons together may form a double bond; (e) Y is selected from the group consisting of C, O, S, NH and a single bond; and (f) E is selected from the group consisting of C(R3)(R4)A, A, and a substituted or unsubstituted group selected from the group consisting of (CH2)n COOR19.
US20120058945 Neuroprotective iron chelators and pharmaceutical compositions comprising them Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, e.g., a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, an inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding aging, and prevention and/or treatment of skin aging and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety. The neuroprotective function is imparted to the compound, e.g., by a neuroprotective peptide. A combined antiapoptotic and neuroprotective function is provided by a propargyl group.
CN1714793A Famciclovir slow-releasing capsule for anti-virus treatment and its producing method The present invention relates to a kind of slow-releasing famciclovir capsule for antiviral treatment, and features that the slow-releasing famciclovir capsule is prepared through coating famciclovir medicine with supplementary material to form the pellet core, coating the pellet core with inner release controlling layer of water insoluble polymer, re-coating with outer release controlling layer of enteric polymer to form release controlling famciclovir pellet, and encapsulating famciclovir pellet to form the slow-releasing famciclovir capsule. In artificial gastric juice and artificial intestinal juice, the slow-releasing famciclovir capsule has its medicine releasing degree of 10-30 %, 30-70 % and over 70 % separately in 1.5 hr, 3 hr and 8 hr. The pellet is measured to have medicine content of 56.8-65.2 %.
CA2319640C Electrochemically reactive cathodes for an electrotransport device The present invention relates generally to improved cathodes (24) for use in an electrotransport device (10) for transdermally or transmucosally delivering a beneficial agent (e.g. a drug) to, or extracting a body analyte (e.g., glucose) from, the body surface of a patient. Most particularly, the present invention relates to a cathodic electrode (24) in the form of a silver halide foil which can be made, e.g., by forging particulate silver chloride. The cathode (24) does not absorb agent (e.g., drug), eliminates the need for binders, solvents and processing aids during the manufacturing process, and increases dimensional freedom of design.
WO2012057291A1 Process for production of phenolic polymerizable compound having physiological activity The present invention relates to a process for producing a phenolic polymerizable compound represented by formula (1) or (2) (wherein X1-X9 independently represent a hydrogen atom, a hydroxy group, a saturated or unsaturated linear or branched alkoxy group having 1-10 carbon atoms, or a saturated or unsaturated linear or branched alkyl group having 1-10 carbon atoms; Y represents a hydrogen atom, a hydroxy group, a saturated or unsaturated linear or branched alkoxy group having 1-10 carbon atoms, a saturated or unsaturated linear or branched alkyl group having 1-10 carbon atoms, or a group represented by formula (6) (wherein X10 and X11 independently represent a hydrogen atom, a hydroxy group, a saturated or unsaturated linear or branched alkoxy group having 1-10 carbon atoms, or a saturated or unsaturated linear or branched alkyl group having 1-10 carbon atoms); and Z represents a hydrogen atom or a group represented by formula (3); wherein X1-X11 may be the same as or different from one another), which is characterized by heating a 4-hydroxysilicic acid compound in the presence of a metal salt.
US20080085904 Heat Shock Protein 90 (HSP90) inhibitors; 5-(2-hydroxy-4-methoxyphenyl)-1-(3-nitrophenyl)-1H-pyrazole for example; antitumor agent, viral diseases, transplant rejection, cystic fibrosis, angiogenesis inhibition, infectious, autoimmune, or inflammatory diseases, ischemia, chemotherapy cytoprotectant Novel 1,5 diphenylpyrazole derivatives of the formula (I), in which R1-R6 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
EP1794115A2 N-ethyl hydroxyethylamines useful in treating cns conditions An N-ethyl hydroxyethyleneamine of formula (I) are disclosed which are useful in treating CNS conditions, including neurodegenerative diseases such as Alzheimer's Disease.
EP2625162A1 Methods of making l-ornithine phenyl acetate Disclosed herein are processes for making L-ornithine phenyl acetate. The process may include, for example, intermixing a halide salt of L-ornithine with silver phenyl acetate. The process may also include forming a phenyl acetate salt in situ. The present application also relates to various compositions obtained from these processes, including crystalline forms.
WO2008015563A2 Salts of rosuvastatin and processes for their preparation Novel salts of rosuvastatin and processes for their preparation are disclosed. Pharmaceutical compositions comprising a therapeutically effective amount of one or more salts of rosuvastatin selected from the group consisting of a barium salt, strontium salt, zinc salt, cesium salt, cadmium salt and mixtures thereof are also disclosed.
CN102526262A Double-fiber tablet and preparation method thereof The invention discloses a double-fiber tablet and a preparation method thereof. The preparation method of the double-fiber tablet comprises the following steps of: (1) weighing polydextrose, hawthorn powder, low-substituted hydroxypropyl cellulose, corn cellulose, gelatin, microcrystalline cellulose and magnesium stearate; (2) sequentially sieving with a 40-mesh sieve and a 60-mesh sieve to enable the particle sizes of the polydextrose, hawthorn powder, low-substituted hydroxypropyl cellulose, corn cellulose, microcrystalline cellulose and magnesium stearate to be 40-60 meshes for later use; (3) adding the gelatin into boiled water, and insulating; (4) putting the polydextrose, hawthorn powder, low-substituted hydroxypropyl cellulose, corn cellulose and microcrystalline cellulose treated in the step (2) into a granulating machine, mixing, injecting gelatin size, granulating and drying; (5) mixing the magnesium stearate with the particles; and (6) tabletting. Through the double-fiber tablet disclosed by the invention, a layer of protective film can be formed in the small intestine, thereby regulating blood fat, reducing fat deposition, preventing obesity and treating constipation.
CN103159815A Monophosphate vidarabine crystalline compound, medical composition and preparation method thereof The invention provides a monophosphate vidarabine crystalline compound, a medical composition and a preparation method thereof. The crystalline compound is good in stability and solubleness, simple in preparation method and higher in bioavailability, and provides a better choice for clinical application of medicines.
CN103720681A Application of tranilast in preparing medicine for preventing pathological scar The invention relates to novel application of tranilast, namely novel application of tranilast in preparing a medicine for preventing pathological scar. A tranilast oral preparation can be used to prevent pathological scar, active prevention as well as prevention and treatment are achieved by advancing treatment time, the pathological scar is inhibited at the source, and the application is an innovation to various traditional treatment technological means, including oral administration of tranilast after scar is formed, on concept and method.
US20100143359 Expression of foxp3 by cancer cells The present invention relates to the treatment, diagnosis, and prophylaxis of cancer based on the expression of foxp3.
WO2013027932A1 Pharmaceutical composition for preventing or treating premature ejaculation comprising 8-hydroxyclomipramine or its salt The present invention provides a pharmaceutical composition for preventing or treating premature ejaculation comprising 8-hydroxyclomipramine or its pharmaceutically acceptable salt as an active ingredient.
US20110212926 Water-soluble acetaminophen analogs The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and/or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided.
EP1337522B1 farnesyl protein transferase inhibitors The present invention describes compounds useful for the inhibition of Farnesyl Protein Transferase. This invention also discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with FPT.
WO2013102665A1 Oromucosal liquid estradiol compositions The present invention relates to low dose estradiol solutions for oromucosal administration suitable in replacement therapy or suppletion of low estradiol levels and also for preventing, alleviating or treating symptoms associated with low endogenous levels of estradiol in female subjects.
EP1599477B1 Sulfonamide substituted xanthine derivatives for use as pepck inhibitors The present invention is concerned with sulfonamide substituted xanthine derivatives of formula (I) or a pharmaceutically acceptable salts or prodrugs thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula (I) and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.
US20080312262 Such as 2-(methylamino)-2-oxoethyl {2-[(4-chlorophenyl)oxy]ethyl}carbamate; sleep disorders The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.
CN101032480A Application of triptolide in the preparing of medicine for curing urinary podocytes glomerulonephritis Wilfodine A is used in treating renal glomerulus podocyte diseases. It can suppress damage on renal glomerulus podocyte and reduce the generation of proteinuria caused by renal glomerulus podocyte diseases, so that it may be used in preparing medicine for treating renal glomerulus podocyte diseases.
CN1763075A Solasodine hydrobromate and its preparation method and its uses in medicine The present invention provides one new kind of compound, solasodine hydronbromide, with obvious anticancer and asthma relieving effects, less toxic side effect, stable property and high dissolubility. The molecular expression is shown. The present invention also relates to the preparation process of solasodine hydronbromide with black nightshade, Australia eggplant or yellowfruit nightshade as material. The preparation process includes acid leaching and precipitating to obtain total alkaloid. The preparation process of the present invention has low reagent cost, no environmental pollution, short production period, high product purity and other advantages. The present invention also relates to the application of solasodine hydronbromide in preparing medicine for treating cancer and relieving asthma, etc.
WO2007132220A1 Combination of a 2-substituted-4-heter0aryl-pyrimidine amine with a cytotoxic drug and use thereof in the treatment of a proliferative disorder A first aspect of the invention relates to a combination comprising (a) a cytotoxic drug selected from: (i) doxorubicin; (ii) SN-38, or a prodrug thereof; (iii) gemcitabine; and (b) a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl; R2 and R3 are each independently selected from H and alkyl; and R4 is a heteroalicyclic group optionally substituted by one or more substituents selected from alkyl, CO-alkyl and aralkyl. Further aspects of the invention relate to pharmaceutical products and therapeutic uses of said combination.
WO2008151389A1 Chemically modified macromolecules The present invention relates generally to chemically modified macromolecules for use in immunotherapy. In particular, the present invention relates to dendrimers having one or more adjuvant groups conjugated to the surface thereof. The invention further relates to combinations comprising a dendrimer having one or more adjuvant groups conjugated to the surface thereof, together with an antigen.
US20100303754 Process for preparation of cyclodextrin oligomers or polymers, products obtained and uses A process for the preparation of cyclodextrin oligomers or polymers, whereby the cyclodextrin molecules are coupled to one another covalently via a spacer arm, based on a coupling reaction between an alkyne and an azide producing the formation of an aromatic heterocyclic bridge between the coupled units. Also described are the cyclodextrin oligomers or polymers that are obtained and their uses.
CN103637992A Cefdinir granular preparation and preparation method thereof The invention relates to a cefdinir granular preparation and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The cefdinir granular preparation contains 80-120 parts weight of a cefdinir crystal form, wherein an X-ray powder diffraction pattern of the cefdinir crystal form has characteristic absorption peaks at reflection angle 2 theta of 12.1 +/-0.2 degrees, 17.5+/- 0.2 degrees, 19.6+/- 0.2 degrees, 21.4+/- 0.2 degrees, 24.7+/- 0.2 degrees, 29.5+/- 0.2 degrees and 31.8+/- 0.2 degrees. The cefdinir granular preparation disclosed by the invention quickens absorption in a human body by using the cefdinir crystal form, and improves bioavailability, so that curative effect is improved; moreover, stability is better, an availability factor of unit dose is improved, and economical and social significances are very high.
US20100137290 Oxazolidinone antibiotic derivatives The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are seleted from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to salts of such compounds.
CN101590043A Compound preparation for treating respiratory tract infection and preparation method thereof The invention relates to a medicinal composition for treating acute and chronic respiratory tract infection, in particular to a compound preparation taking amoxicillin and ambroxol hydrochloride as active components and a preparation method thereof. The formulation comprises capsules and tablets. In the prescription, medicinal active components contain the amoxicillin and the ambroxol hydrochloride, and excipients comprise a disintegrant, a filling agent, a glidant and an adhesive. The compound preparation supplements the specification dosage of a product which is on the market, namely an oral solid preparation, overcomes the disadvantage that the divided dose is not accurate when children take, is particularly suitable for the children to take, and greatly improves the adaptability of drug use of child patients.
EP1207861B1 Treatment of fungal infections utilizing a fungal growth medium The present invention relates to a method of treating a topical fungus infection on a mammal comprising the steps of: topically applying to said fungus an amount of a fungal growth medium effective to induce said fungus from the dormant state into the vegetative state; and administering to said mammal a therapeutically effective amount of an antifungal agent.
US20100119622 3h-benzooxazol-2-one modulators of d2 receptor and/or 5-ht1a receptor The present invention relates to new 3H-benzooxazol-2-one modulators of D2 receptors and/or 5-HT1A receptors, pharmaceutical compositions thereof, and methods of use thereof.
CN102988337A Histone deacetylase inhibitor and application thereof The invention discloses a histone deacetylase inhibitor, and application of the histone deacetylase inhibitor in preparation of a medicament with a function of inhibiting the liver cancer. The histone deacetylase inhibitor is L-carnitine, can inhibit the activity of histone deacetylase (HDAC), and can be used as the medicament for inhibiting the liver cancer.
US20080318932 Sodium Channel Blocker Compositions and the Use Thereof Methods of treating or preventing chronic pain or convulsion are disclosed by administering to an animal a sodium channel blocker and at least one of gabapentin and pregabalin. Also disclosed are pharmaceutical compositions and kits for the treatment or prevention of chronic pain or convulsion.
CN1927172A Anticancer slow release agent comprising tetrazole violet and potentiating agent thereof Disclosed is a slow release injection agent containing tetrazole lonone and synergistic agent, which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents being the combination of tetrazole lonone and tetrazole lonone synergistic agent selected from topoisomerase depressant and/or tetrazines compounds, the slow release auxiliary materials are selected from Polifeprosan, sebacylic acid copolymer, EVAc, D, L-polylactic acid and copolymer, polyethylene glycol mono methyl and copolymer, polyethylene glycol / polylactic acid copolymer, hydroxy-terminated polylactic acid, or one of hydroxy-terminated polylactic acid / glycollic acid copolymer or their combination, the viscosity of the suspension adjuvant is 100-3000cp and is selected from sodium carboxymethylcellulose. The slow release microspheres can also be prepared into slow release implanting agent for injection or placement in or around tumor, the period of local drug release can be about 30-50 days, as a result, the injection can be used for the treatment of tumor independently, and has the functions of improving the treatment effect of the non-operative methods such as chemotherapy and/or radiotheraphy.
WO2010090546A1 Composition of amino acids for sublingual applying for enhanced skin integument repigmentation in vitiligo and method of its administration The task of this invention is in use of composition containing natural metabolites - amino acids, and in method of its administration which make it possible to increase skin repigmentation through sulfurcontaining compounds rise and activation of endogenic metabolic reactions, and to get persistent normalization of melanogenesis thus improving skin integument and as a consequence patient's quality of life. Composition includes L cystine, L glutamic acid and glycine in the following quantity, mg: L cystine 85 ± 10%, L glutamic acid 85 ± 10%, Glycine 85 ± 10%. The amino acid composition mentioned above must be administered 3 times a day for 5 weeks independent of meal in accordance with method of increase of skin integument repigmentation in vitiligo. The course can be repeated in 4-5 weeks.
WO2007097301A1 Prophylactic or therapeutic agent for cerebral ischemia or cerebral ischemic reperfusion injury in stroke Disclosed is a prophylactic or therapeutic agent for cerebral ischemia injury or cerebral ischemic reperfusion injury occurring in stroke such as cerebral infarction or cerebral hemorrhage, which develops its efficacy through a mechanism different from those of conventional ones and can be administered over a long period. The prophylactic or therapeutic agent comprises 6-fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2- carboxamide as an active ingredient. Particularly preferably, the compound is fidarestat, which is an optically resolved form having a (2S,4S) configuration.
WO2007066642A1 Oral preparation for preventing or improving skin dryness It is intended to provide an oral preparation for preventing or improving skin dryness accompanying atopic dermatitis, xeroderma, rough hands, rough skin, or the like. According to the invention, the oral preparation for preventing or improving skin dryness comprising citrulline or a salt thereof as an active ingredient can be provided.
WO2012047017A3 2,3-dihydro-isoindol-1-one derivative and a composition comprising the same The present invention relates to a pharmaceutical composition for the treatment, alleviation or prevention of diseases associated with abnormal or deregulated kinase activity, the composition comprising a compound represented by chemical formula 1 and a pharmaceutically acceptable salt, hydrate, prodrug or solvate thereof. The compound and composition of the present invention inhibit various types of protein kinase activity, and hence can be used to advantage in the treatment, alleviation or prevention of diseases associated with abnormal or deregulated kinase activity.
WO2007065595A3 Xanthine derivatives, processes for preparing them and their uses The present invention concerns xanthine derivatives, having formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
CN103211953A Preparation method of medicine for promoting fracture healing The invention discloses a preparation method of a medicine for promoting fracture healing. The preparation method comprises the following steps of: adding pollen typhae, Japanese chloranthus root rhizome extraction volatile oil, black false hellebore and borneol ultrafine powder in a water extract of Circium japonicum, rheum officinale, Chinese Polyphaga, gallnut and Japanese calystegia; and uniformly stirring and decompressing and concentrating. Clinical experiments show that the medicine provided by the invention has the characteristics of good curative effect and high safety when used for promoting fracture healing and is worthy of clinically applying and popularizing.
WO2007038788A3 Small interfering rnas as non-specific drugs The present invention is directed to a method of modulating {e.g., inducing, inhibiting) activation of a double stranded RNA (dsRNA) signaling pathway, such as the dsRNA signaling pathway that accompanies RNA interference (RNAi) of a target RNA sequence, in a cell, comprising introducing into the cell small interfering RNA (siRNA) that degrades the target RNA sequence, and maintaining the cell under conditions in which RNAi of the target RNA sequence occurs and activation of the dsRNA signaling pathway is modulated in the cell.
EP1695977A2 Spiro [isobenzofuran-1,4'piperidin]-3-ones and 3H-spiroisobenzofuran-1, 4'-piperidines This invention relates generally to substituted spiro[isobenzofuran-1,4'-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4'-piperidines that are modulators of mammalian neuropeptide Y5 (NPY5) receptors, and to the use of such compounds for treating a variety of physiological disorders associated with NPY5 receptor activation, such as feeding disorders, psychiatric disorders and cardiovascular diseases. The invention further relates to the use such compounds as probes for the detection and localization of NPY5 receptors.
US20100209447 Methods of making and using a cell penetrating peptide for enhanced delivery of nucleic acids, proteins, drugs, and adenovirus to tissues and cells, and compositions and kits A peptide-POD with ability to penetrate and deliver fluorophores, siRNA, DNA and quantum dots to cells in culture and retinal and ocular tissues in vivo is provided herein. POD couples to adenovirus vectors, enhancing tropism for certain cells, potentially providing a safer and more efficacious method to deliver molecules to ocular and other tissues in vivo. POD constructs are therapeutic delivery vehicles for treating cells and tissues, including ocular cells and tissues suffering from retinal degeneration.
WO2008065155A1 Cdk inhibitors for treating pain The present invention relates to methods of preventing and/or treating any type of pain comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases.
WO2010119264A1 Imidazopyrazines for use as kinase inhibitors There is provided compounds of formula (I), wherein R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
CN101496804A Composition containing tripterine, preparation method and use The invention discloses a composition of celastrol and arginine salts and a preparation method and application thereof. The medicine composition obtained by the method has better stability and water-solubility compared with the celastrol. The invention also provides the application of the medicine composition in preparing a medicine for treating tumor.
EP2574171A1 Repair of fragmented dna and treatment of heavy metal intoxication by intravenous injection of nano-hydroxyapatite Synthesis of nano-hydroxyapatite by an organic-inorganic complexion route. Such material was injected intravenously into rats after the exposure of these rats to LD50 of toxic heavy metal. The prepared nano-hydroxyapatite success in repair the fragmented DNA within 48 hours after injection with single dose only without any side effects. Also, heart, liver and thyroid function enzymes were evaluated and the results confirmed the bio-safe usage of this made material. Therefore, the prepared nano-hydroxyapatite can be use safely as a thereby by intravenous injection with suitable doses for different diseases such as cancer, poising and osteoporosis.
EP1200126B1 Use of cd28 specific monoclonal antibodies for producing a pharmaceutical composition for treating virus infections The invention relates to the use of monoclonal antibodies which are specific for CD28 and activate the T lymphocytes of several up to all subgroups without the occupation of an antigen receptor of the T lymphocytes and which therefor activate said lymphocytes in an antigen unspecific manner or the invention relates to the use of an analogue thereof for producing a pharmaceutical composition in the form of a preparation or a preparation packet for treating virus infections in humans or lower warm-blooded animals having infected T lymphocytes. The pharmaceutical composition additionally contains a virus inhibitor. The invention also relates to a corresponding pharmaceutical composition and a treatment plan including the pharmaceutical composition.
DE102007049630A1 New amide compounds used for therapy and/or prophylaxis of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy Amide compounds (I), are new. Amide compounds of formula (I), are new. q : 0 or 1; R 1>mono or bicyclic 6-12C aryl, 5-12 membered hetero aryl, 3-10C cycloalkyl, or 3-10 membered hetero cycloalkyl residue, which is unsubstituted or substituted up to 3 residue, where the substituents are 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, partialy or completely fluorinated 1-6C alkyl or alkoxy, 1-6 alkoxy-1-6C alkyl, 1-6C aIkoxy-1-6C alkoxy, -(CH 2) pC 3-C 10 cycloaIkyl, -(CH2) p heterocycIo alkyl, -(CH 2) pCN, -(CH 2) pHaI, -(CH 2) pNO 2, (CH 2) pC 6-C 12 aryl with Z substituent, -(CH 2) p-heteroaryl with Z substituent, -(CH 2) pPO3(R 4>) 2, -(CH 2) pNR 5>R 6>, -(CH 2) pNR 7>COR 4>, -(CH 2) pNR 7>CSR 4>, -(CH 2) pNR 7>S(O)R 4>, -(CH 2) pNR 7>S(O) 2R 4>, -(CH 2) pNR 7>CONR 5>R 6>, -(CH 2) pNR 7>COOR 4> -(CH 2) pNR 7>C(NH)NR 5>R 6>, -(CH 2) pNR 7>CSNR 5>R 6> -(CH 2) pNR 7>S(O)NR 5>R 6>, -(CH 2) pNR 7>S(O)2NR 5>R 6>, -(CH 2) pCOR 4>, -(CH 2) pCSR 4>, -(CH 2) pS(O)R 4>, -(CH 2) pS(O)(NH)R 4>, -(CH 2) pS(O) 2R 4>, -(CH 2) pS(O) 2NR 5>R 6>, -(CH 2) pSO 2OR 4>, -(CH 2) pCO 2R 4>, -(CH 2) pCONR 5>R 6>, -(CH 2) pCSNR 5>R 6>, -(CH 2) pOR 4>, -(CH 2) pSR 4>, -(CH 2) pCR 4>(OH)-R 4>, -(CH 2) pC=NOR 4>, -O-(CH 2) n-O-, -O-(CH 2) n-CH2-, -O-CH=CH- or -(CH 2) n+2 ->, where n=1 or 2; p : 1,2,3,4,5 or 6; Z : cyano, halogen, nitro, -(CH 2) pOR 4>, -(CH 2)S(O) 2R 4>, -C(O)R 4>, -CO 2R 4>, -O-R 4>, -S-R 4>, -SO 2NR 5>R 6>, -C(O)-NR 5>R 6>, -OC(O)-NR 5>R 6>, -C=NOR 4>, -NR 5>R 6> or partially or completely fluorinated 1-6C alkyl or alkoxy; R 4>H, 1-6C alkyl, 1-3C hydroxy alkyl, 1-3C alkoxy-1-3C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C, cycloalkyl, 6-12C aryl or partialy or completely fluorinated 1-3C alkyl; R 5> and R 6>H, with W' substituent 1-6C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C cycloalkyl, 6-12C aryl or a hydroxy group, where W'=NR 8>R 9>; R 8>H or 1-3C alkyl; R 9>H or 1-3C alkyl; R 5>hydroxy group; R 6>H, 1-6C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C cycloalkyl or 6-12C aryl; R 7>H, 1-6C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C cycloalkyl or 6-12C aryl; R 2>mono or bicyclic 6-12C aryl, 5-12 membered hetero aryl reidue, which is unsubstituted or substituted up to 3 residue as specified under R 1>, preferably phenyl or naphthyl substituted derivatives; R 3>a group of formula (i)-(xx); R 5a>, R 5b>H or alkyl optionally at least partially substituted by F, or R 5a> + R 6a> + attached atoms : 3-6 membered ring, and R 4a>H or 1-4C alkyl optionally at least partially substituted by F. An independent claim is also included for a pharmaceutical composition which comprises compound (I), an additional active subsatance i.e. selective estrogen receptor modulator and a pharmaceutically acceptable carrier. [Image] [Image] [Image] [Image] - ACTIVITY : Gynecological; Analgesic; Cytostatic. - MECHANISM OF ACTION : Progesterone receptor modulators.
CN103340858A Dolasetron composition for injection The invention provides a dolasetron composition for injection and relates to the technical field of medicaments and medicament manufacturing. The main medicaments of the composition are dolasetron and melatonin, wherein the melatonin comprises a quick release part and a slow release part contained in cyclodextrin. The dolasetron composition for injection provided by the invention can be used for improving the treatment effect of the dolasetron, avoiding instability, quick distribution and elimination and the like of MT ((Metal Thionein) caused by oral absorption, reducing the first-pass effect of the MT and reducing the dosage of the dolasetron. The medicament administration design combining the quick release with the slow release satisfies physiological secretion characteristics of the MT, can be used for solving the problem that the half-life period of the MT is short, increasing the biological utilization rate of the dolasetron composition, and achieving the synergism of the dolasetron for treating CINV (Chemotherapy Induced Nausea And Vomiting). The quick release part and the slow release part are combined, so that not only can the CINV be treated, but also the treatment effect of the dolasetron on the CINV can be improved, and therefore, the treatment course is shortened, the dosage of the dolasetron is reduced, the side effect of the dolasetron is lowered, and the body immunity can be improved. A certain concentration of melatonin is kept in the blood of the human body, so that the stress response of the organisms can be effectively lowered for facilitating the treatment of the CINV.
WO2006055659A2 Fixed dose combination op dutasteride and tamsulosin Pharmaceutical compositions that include a steroid 5-alpha reductase inhibitor in a fixed dose combination with an alpha adrenergic blocker are described.
WO2007096334A1 Pyrrolopyrrolones active as kinase inhibitors Compounds represented by formula (I) wherein A, R1, R2, R3, and R4 are as defined in the specification, compositions thereof, and methods of use thereof.
EP1325002B1 1,2,5,10-tetrahydropyridazino¬4,5-b|quinoline-1,10-diones and their use for the treatment of pain Compounds useful for the treatment of pain in accord with structural diagram (I), or tautomers or pharmaceutically-acceptable salts of such compounds, wherein R1 and A are as disclosed in the specification. Also disclosed are methods for the treatment of pain using compounds according to structural diagram (I) and pharmaceutical compositions comprising compounds according to structural diagram (I).
CN101113158A siRNA disturbing RdRp gene function of SARS virus The invention discloses two anti-SARS-coV siRNA and applications thereof. The anti-SARS-coV siRNA of the invention is of obvious functional effect, and can be acquired through establishing siRNA expression box, which overcomes the problem of high price of chemical synthesized siRNA, and plays an important role in the prevention work of SARS-coV.
US20080261931 Method and Means of Preventing and Treating Sleep Disordered Breathing A method of treating or preventing snoring, obstructive sleep apnea (OSA) and/or central sleep apnea (CSA) comprises administering a pharmacologically effective amount a salt of acetylhomotaurine (AcHT) such as calcium acamprosate (CA) to a patient. Also disclosed is the use of AcHT and CA for the manufacture of a medicament for treating or preventing snoring, OSA and/or CSA and of a diagnostic device, kit or composition; a protective patch comprising AcHT or CA; and a pharmaceutical composition comprising AcHT or CA and an agent capable of alleviating the effects of snoring OSA and/or CSA, in combined amounts effective in the treatment of snoring OSA and/or CSA, and a carrier.
USRE40793 treating conditions related to impairment of gastric emptying, gastromotility disorders; superior gastrokinetic properties; e.g. trans-4-amino-N-[(1-butyl-3-hydroxy-4-piperidinyl)methyl]-5-chloro-2,3-dihydro-7-benzofurancarboxamide The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C (═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ring-system; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
WO2011005595A2 2-5a analogs and their methods of use Disclosed herein are compounds that activate RNaseL, methods of synthesizing compounds that activate RNaseL and the use of compounds that activate RNaseL for treating and/or ameliorating a disease or a condition, such as a viral infection, a bacterial infection, cancer and/or parasitic disease.
CN103118658A Collagen production promoter, hyaluronic acid production promoter and wrinkle ameliorating agent The present invention addresses the problem of providing a collagen production promoter, a hyaluronic acid production promoter and a wrinkle ameliorating agent which contain dehydrocostuslactone.
US20100120898 MicroRNA Expression Signature for Predicting Survival and Metastases in Hepatocellular Carcinoma Provided herein are methods and compositions for the diagnosis, prognosis and treatment of Hepatocellular carcinoma (HCC). Also provided are methods of identifying anti-HCC agents.
US20090297601 Dosage form time-lagged of drugs for the therapy of insomnia The invention is concerned with methods and compositions for treating insomnia, and provides a dosage form containing a drug substance useful in the treatment of insomnia, the dosage form being adapted to release said drug substance after a lag time during which substantially no drug substance is released, the lag time being about at least one hour after administration of the dosage form.
WO2012178022A3 Therapeutic applications targeting sarm1 The present disclosure provides methods for reducing axonal and/or synaptic degradation in neurons by modulating sterile α/Armadillo/Toll-Interleukin receptor homology domain protein (SARM) activity and/or expression.
WO2009125117A3 Dermatological composition that can be used in particular for the care and prevention of eschars The invention relates to a composition formulated for a topical application to the skin containing, as essential constituents, peroxide lipids that have a degree of peroxidation between 30 and 500 milliequivalents per kg of peroxide lipids and cod liver oil. This composition can be used as a medical device, in order to form a protective film on the skin, especially for the care of irritated skin and/or skin that has red spots and/or skin that has superficial lesions, and/or as an adjuvant in skin massaging operations. It is most particularly useful for the care and/or prevention of eschars.
US20100010099 Medium and device for proliferation of stem cells and treatment of cancer-related stem cell with resveratrol The invention relates to a device for selecting stem cells with a serum free medium for amplification of stem cells. The invention also relates to a method of treating or preventing diseases caused by cancer-related stem cells. The invention further provides a method of enhancing radiosensitivity of cancer-related stem cells comprising radiotherapy with resveratrol, and the cancer-related stem cell has stronger drug resistance. The present invention further provides that resveratrol promotes differentiation and inhibits teratoma/tumor formation in induced pluripotent stem cells (iPS) and embryonic stem cells
US7271260 3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and method of preparing the same The present invention relates to 3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and a method of preparing the same. The present invention further relates to a composition comprising the same. The composition comprising the 3,4-dihydroquinazoline derivatives of the present invention can be effectively used for preventing and treating angina pectoris, high blood pressure, myocardial disease, pain and epilepsy by blocking the T-type calcium channel.
CN102526697A Piracetam cerebroprotein hydrolysate dropping pill and preparation method thereof The invention belongs to the technical field of medicines and discloses a piracetam cerebroprotein hydrolysate dropping pill and a preparation method thereof. The dropping pill comprises active ingredients and a substrate, wherein the active ingredients are composed of piracetam, cerebroprotein hydrolysate, and the like. The prescription of the dropping pill provided by the invention is confirmed according to a scientific screening test. A pharmacologic test proves that the dropping pill provided by the invention has better pharmacologic effect than that of the marketed preparation taking compound piracetam and cerebroprotein hydrolysate as raw materials.
CN1813769A Ciclesonide oral ulcer paster and its preparing method The present invention relates to a sticking tablet for curing stomatocace. Its adhesive layer contains 0.01-2mg of cyclosonide. Said oral sticking tablet can be general single-layer tablet, also can be double-layer tablet including medicine adhesive layer and water-proof protective layer, its adhesive material mainly is selected from hydroxypropyl methyl cellulose, carbopul, carboxymethylcellulose sodium, hydroxypropyl cellulose and polyvinylpyrrolidone.
WO2013141586A1 Novelpyridopyrimidine derivatives and use thereof The invention provides novel substituted pyridopyrimidines represented by the Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3 OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.
US20120219597 Pharmaceutical formulations for indibulin In certain embodiments, the invention relates to pharmaceutical formulations of an indolyl-3-glyoxylic acid derivative or a pharmaceutically acceptable salt thereof, such as indibulin. Methods of preparing such formulations and methods of treatment using these formulations are also described.
CA2840626A1 Methods of treating recurrent meibomian glands disorder and thereby decreasing the frequency of recurrence A method of treating a recurring meibomian gland disorder in a patient, includes administering to a patient suffering from recurring meibomian gland disorder a composition comprising a therapeutically effective amount of an azalide antibiotic and a glucocorticoid. The method may thereby reduce the frequency of recurrence of the meibomian gland disorder.
CN103565829A Method for improving silkworm cocoon yield stability The invention discloses a method for improving silkworm cocoon yield stability, which comprises the following steps: (1), a mixture composed of virazole, terbinafine hydrochloride and ammonium chloride is used to prepare an aqueous solution according to the mass fraction of 10-15 to 3-7 to 75-85; (2), after the prepared aqueous solution is sprayed to mulberry leaves, mulberry leaves are dried in the air; (3), the mulberry leaves obtained in the step (2) are used for feeding silkworms. According to the invention, by adding the aqueous solution of the mixture composed of virazole, terbinafine hydrochloride and ammonium chloride, prevention and treatment for diseases of the silkworms, such as nuclear polyhedrosis virus, cytoplasmic polyhedrosis and white muscardine, can be achieved, the problem of silkworm cocoon yield reduction caused by the diseases can be solved, and the silkworm cocoon yield stability is ensured.
US20090048227 Substituted-1-Phthalazinamines As Vr- 1 Antagonists Substituted piperidine compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
EP2696868A1 Nutritional compositions including branched chain fatty acids and methods of using same Nutritional compositions for improving, treating and/or preventing various medical conditions and methods of using same are provided. The medical conditions may include allergies, autoimmune diseases, among others. The nutritional compositions include branched chain fatty acids and may include other functional ingredients such as, but not limited to probiotics, nucleotides and amino acids. Methods of administering such nutritional products to individuals in need of same are also provided.
US20100130519 Combination therapy comprising azd2171 and azd6244 or mek-inhibitor ii The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with AZD6244 or MEK Inhibitor II; to a pharmaceutical composition comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II; to a combination product comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II; to the use of AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.
CN102743350A Methionine-vitamin B1 composition injection The invention provides a methionine-vitamin B1 composition injection comprising 5-20 parts by weight of methionine and 1 part by weigh of vitamin B1 and further comprising antioxygen Vc or cysteine. The invention also provides a preparation method of the methionine-vitamin B1 composition injection. The preparation method comprises the following steps: heating water for injection to 40-70 DEG C, then adding methionine in the heated water for injection for dissolving; cooling the temperature of the solution to 30 DEG C, then adding vitamin B1, stirring for dissolving vitamin B1, adjusting the pH value to be 4.0-4.5; and adding activated carbon, filtering, filling filtrate in a bottle and freeze-drying. The product quality of the methionine-vitamin B1 composition injection is superior to thequality of the similar products; moreover, the methionine-vitamin B1 composition injection has the advantages of low impurity content and good stability.
US20090076057 Deuterium-enriched dutasteride The present application describes deuterium-enriched dutasteride, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2011019617A2 Vitamin d3 and analogs thereof for treating alopecia The invention provides methods and pharmaceutical compositions for preventing or treating alopecia, such as chemotherapy-induced alopecia (CIA). The pharmaceutical compositions of the invention comprises an effective amount of a vitamin D compound in a formulation that topically delivers the vitamin D compound to the epidermis layer but substantially avoids the dermis layer. In chemotherapy patients, the pharmaceutical compositions of the invention can be administered either before or concurrent with the chemotherapy medication.
US7449472 Methods of inhibiting p38 with substituted bicyclic pyrimidines The present invention discloses compounds corresponding to the formula wherein A, X, Y, R, R1 and R2 are as defined within, pharmaceutical formulations, methods of making and uses thereof.
US20070270376 Combinations of Hyaluronic Acid and Polyunsaturated Fatty Acids A pharmaceutical or veterinary composition comprises a hyaluronic acid or a salt thereof or an ester of hyaluronic acid with an alcohol of the aliphatic, heterocyclic or cycloaliphatic series, or a sulphated form of hyaluronic acid, together with at least one eicosanoid or tetraenoic polyunsaturated fatty acid or an ester or a salt thereof, preferably in the form of an extract of fatty acids from the New Zealand Green Lipped Mussel Perna canaliculus. The compositions are active against inflammatory conditions including osteoarthritis.
CN101829126B Application of 3-carbethoxy phenyl-beta-D-glucoside in treating chronic neuropathic pains The invention relates to 3-carbethoxy phenyl-beta-D-glucoside, or a pharmaceutically acceptable salt, ester or solvate thereof and application in preparing medicaments for treating neuropathic pains, wherein a glycosyl part is arbitrary pyranose or furanose; and a representative compound is 3-carbethoxy phenyl-beta-D-acylated xyloside the structural formula of which is disclosed in the specification. On a classical sciatic nerve chronic compression injury (CCI) model, through single intragastric administration and continuous intragastric administration for 7 days, the compound shows definite treatment effect on resisting nervous pains. At a dose point appointed by an experiment, the compound can obviously improve the mechanical stimulus pain threshold, the nervous pain resistant efficacy is equivalent to that of Gabapentin which is a contrast medicament, and the duration is superior to that of the Gabapentin. Proved by research results, the compound can be used for treating the chronic neuropathic pains.
US20120289486 Treatment of eyelid dermatitis A method for the treatment of eyelid dermatitis and/or dermatitis of the periorbital area is provided.
EP1831191B1 Chroman derivatives and their use as 5-ht receptor ligands Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1, R2, R3 and R4 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula (I).
WO2014100615A1 Chimeric antigen receptor-expressing t cells as anti-cancer therapeutics Cytotoxic lymphocytes expressing chimeric antigen receptors (CAR) that target and bind small conjugate molecules (SCM) are disclosed, as well as methods of using the cells and the SCMs in the treatment of cancer.
US7875590 using an injectable or implantable rod-shaped formulation for delivery of osteogenic proteins to treat osteoporotic and/or osteopenic bone; bone morphogenic proteins Methods of using an injectable or implantable rod-shaped formulation for delivery of osteogenic proteins to treat osteoporotic and/or osteopenic bone are disclosed. The formulation comprises hyaluronic acid derivatives and osteogenic proteins, and optional excipients and active ingredients such as a bone resorption inhibitor.
CA2318008C Solid oral pharmaceutical formulation of modified release that contains an acid labile benzimidazole compound The pharmaceutical formulation consists of a number of pellets that comprise a inert nucleus, a layer with the active ingredient, one or more intermediate layers that comprise at least a system of modified release, and an external layer of enteric coating.These pellets can be obtained applying the different layers by means of fluid bed coating techniques using aqueous solutions or suspensions of the components of such layers. The pharmaceutical formulations can be hard gelatine capsules or tablets and are suitable for use in the prevention and treatment of disorders related to abnormal gastric acid secretion.
CN101269223B Anthracene nucleus medicament nano-preparation, preparation method and application thereof The invention belongs to the biomedicine technology field, in particular relates to a new nano-preparation of anthracene-ring medicine, such as adriamycin, etc. and a preparation method thereof. The preparation is composed of anthracene-ring medicine such as adriamycin, nucleic acid, and cationic compound. The specific preparation process is that the anthracene-ring medicine is compounded with the nucleic acid firstly, and then is compounded with the cationic compound to form nano-granule. The preparation reduces the physiological toxicity of anthracene-ring medicine without reducing the anti-cancer activity, has tumor targeting characteristic and can be prepared into tumor-treating medicine.
US20050043214 Antiglaucomatous agent and use thereof The present invention relates to pharmaceutical compositions based on antiglaucomatous active ingredients and to the use thereof for the treatment of glaucomas. The compositions comprise lactalbumin hydrolysate or a fraction thereof. Substantially lower doses of the antiglaucomatous agents are thus possible than is conventionally necessary to achieve a particular antiglaucomatous effect.
US20110237581 Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
EP1000158B1 Endogenetic retroviral sequences, associated with autoimmune diseases or with pregnancy disorders The invention concerns a genomic retroviral nucleic material, in isolated or purified state, at least partially functional or non-functional, whereof the genome comprises a reference nucleotide sequence selected from the group including sequences SEQ ID Nos: 1 to 15, their complementary sequences, and their equivalent sequences, in particular the nucleotide sequences having, for every series of 100 contiguous monomers, at least 70 % and preferably at least 90 % homology with said sequences SEQ ID Nos: 1 to 15. The invention also concerns the application of said material.
US7393524 Baculovirus vectors comprising a capsid polypeptide fused to a GNRH polypeptide The invention relates to a genetically engineered baculovirus wherein said virus is engineered to target therapeutic agents to cells, typically cancer cells, for example prostate cancer cells.
US20120213765 Method and composition mitigating fecal and flatulent odors A method of mitigating or eliminating the odor associated with the feces or flatulence of an animate subject, whether human or animal, by means of administering activated carbon, whether alone or in composition with further inert ingredients, to the subject for ingestion and digestion of the same in advance of the subject either defecating or expelling flatulence.
CN102827736A Health-care wine for reducing fever and causing diuresis The invention relates to a health-care wine for reducing fever and causing diuresis. The health-care wine is prepared by the following steps: preparing a dispensed medicine by mixing raw materials of: by weight, 15 parts of talcum, 13 parts of broom cypress fruit, 15 parts of imperata rhizome, 12 parts of achyranthes root, 17 parts of Herba Lopatheri and 15 parts of Akebia Fruit; grinding the dispensed medicine and immersing in 1L of pure grain spirit; shaking once every day; sieving through a sieve of 200 meshes after 30 days, filling and sealing, and sterilizing to prepare the health-care wine for reducing fever and causing diuresis. The health-care wine for reducing fever and causing diuresis requires a simple preparation method, is convenient to drink, has effects of clearing heat, dehumidifying and causing diuresis, and can clear heat, cause diuresis and ease urine if drunk for a long time.
CN101659706B Method for purifying and separating X-fraction polysaccharide from fruit bodies or mycelia of polyporus frondosus The invention relates to a method for purifying and separating X-fraction polysaccharide from the fruit bodies or mycelia of polyporus frondosus, which is characterized in that: crude polysaccharide extracted from the fruit bodies or the mycelia of the polyporus frondosus is subjected to complex reaction and primary purification, and is deproteinized by a sevag method, and then X-fraction pure polysaccharide of the polyporus frondosus is prepared by a graded ethanol precipitation method. The polysaccharide has good effect of reducing blood fat. The crude polysaccharide is obtained by a water extraction and ethanol precipitation method, and is separated and purified according to different natures of a complex compound and the X-fraction polysaccharide to ethanol precipitation concentration. The method has convenient operation, obtains the target product with high purity, and provides a feasible way for producing the X-fraction polysaccharide of the polyporus frondosus on a large scale,and preparing various medicaments and health-care foods.
CN103142770A Compound houttuynia cordata lotion and preparation method thereof The invention discloses compound houttuynia cordata lotion. The lotion consists of the following components in parts by weight: 120 parts of houttuynia cordata, 80 parts of corydalis tuber, 80 parts of mirabilite, 80 parts of Chinese rhubarb, 60 parts of golden cypress, 60 parts of dandelion, 40 parts of radix sophorae flavescentis, 40 parts of Chinese violet, and 3.0 part of sodium benzoate. The compound houttuynia cordata lotion is reasonable in prescription and has a good effect.
CN102796121A 3-aryl-7H-thiazol[3,2-b]-1,2,4-triazinyl-7-one derivatives and application thereof The invention discloses 3-aryl-7H-thiazol[3,2-b]-1,2,4-triazinyl-7-one derivatives and application thereof, particularly 3-aryl-7H-thiazol[3,2-b]-1,2,4-triazinyl-7-one derivatives disclosed as general formula I or pharmaceutically acceptable hydrates and salts thereof, and application in enhancing memory of patients with dementia and Alzheimer's disease. In the general formula I, R1 and R2 are respectively and randomly one or two or three of H, halogens, hydroxy group, methoxy group, methyl group, nitro-group, -O(CH2)n1NR3R4 and -O(CH2)n2CONR5R6; R3, R4, R5 and R6 are respectively selected from methyl group, ethyl group, pyrrolidinyl group formed by the methyl or ethyl group and nitrogen atom connected with the methyl or ethyl, methylpyrrolidinyl group, dimethylpyrrolidinyl group, piperidyl group, morpholinyl group or hexamethylene imino group ring; n1 is a whole number ranging from 2 to 6; n2 is a whole number ranging from 1 to 6; and X is O or S.
WO2014000686A1 Pyrimidobenzoazepine compound and use thereof as antitumour drug Disclosed in the present invention are a Pyrimidobenzoazepine compound and the use thereof as an antitumour drug. The advantage of the present invention consists in that the compound and the pharmaceutical agent thereof have good effects on treating diseases caused by gene expression abnormity, such as tumours, endocrine disturbance, immune system diseases, genetic diseases and nervous system diseases. When used as an antitumour drug, it has a stronger antitumour activity and lower toxic side effects, and is more easily used as an antitumour drug. The compound containing pyrimidobenzoazepine is the compound of formula (I) and the pharmaceutically acceptable salts thereof.
EP0966283B1 Pharmaceutical products for curing and preventing diseases resulting from the damaging of the vascular endothelial cells The invention relates to the use of certain hydroxylamine derivatives in the therapy or prevention of illnesses connected with the dysfunction of the vascular endothelial cells. Another object of the invention is the use of the same compounds in the preparation of pharmaceutical compositions against the above diseases. In general formulae (I) and (II), R<1> and R<2> independently refer to a hydrogen atom or a straight or branched alkyl group of 1 to 6 carbon atoms, or R<1> and R<2> together with the nitrogen atom in-between form a saturated 5 - 7 membered heterocyclic group, containing optionally further nitrogen and/or oxygen heteroatoms, A refers to a straight or branched alkyl group of 4 to 12 carbon atoms, a phenyl group, substituted or unsubstituted, containing preferably an alkyl-, haloalkyl- or nitro group as substituent, or a 5 - 6 membered heteroaromatic ring containing nitrogen, oxygen or sulphur, in general formula (I), Z refers to a covalent bond, and in general formula (II) to a covalent bond or a =NH group, in general formula (I), X refers to a halogen atom or to a - NR<3>R<4> group, wherein R<3> and R<4> independently refer to a hydrogen atom or a straight or branched alkyl group of 1 to 6 carbon atoms, while in general fomrula (II) X refers to an oxygen atom, in general formula (II), R' refers to a hydrogen atom or a straight or branched alkyl group of 1 to 6 carbon atoms, and in general formulae (I) and (II), Y refers to a hydrogen atom, a hydroxyl group or an acyloxy group, which contains preferably the acyl part of a long chain fatty acid of 8 to 22 carbon atoms, or of a cyclic aromatic carboxylic acid as its acyl component, and in the compounds of general formula (I) wherein X refers to a - NR<3>R<4> group and Y refers to a hydroxyl group, the X group is condensed with the Y substituent and forms the intramolecular ring represented by general formula (III), in which formula A, Z, R<1> and R<2> have the same reference as above.
CA2141652C Fluorinated vitamin d3 derivative This invention is for 1.alpha.-fluoro-25-hydroxy-16-ene-23-yne-cholecalciferol, which can be further characterized by the formula: and which is useful as an agent for the treatment of sebaceous gland diseases such as acne and sebhorreic dermatitis. It can be prepared by removing the silyl protecting groups from a corresponding compound with silyl protected hydroxy groups.
CN101054604A Application of oligonucleotide complemented with rna used as transcription product of gene Susceptibility of a tumor cell to an anticancer agent is tested by measuring an expression level or levels of a gene or genes selected from the group consisting of the genes listed in Tables 3 and 4 in a tumor cell collected from a cancer patient treated with an anticancer agent (E7070 and related compounds thereof), or causing the anticancer agent to act on a tumor cell collected from a cancer patient and measuring an expression level or levels of a gene or genes selected from the group consisting of the genes listed in Tables 3 and 4 in the tumor cell, and determining that the tumor cell is susceptible to the anticancer agent when the expression level or levels of the gene or genes listed in Table 3 increase, or the expression level or levels of the gene or genes listed in Table 4 decrease.
CN103690967A Autonomous cattle feeding drug carrier and preparation method thereof The invention relates to an autonomous cattle feeding drug carrier and a preparation method thereof. The drug carrier comprises the following components by mass percent: 15-30% of banana, 20-30% of corn flour, 0.4-8% of carageenan, 5-15% of soybean protein, 2-8% of honey, 0.05-0.5% of citric acid, 0.1-2% of vitamin complex, 0.1-2% of complex mineral, 0.02-0.05% of potassium sorbate, and 32-55% of moisture. The drug carrier is suitable for direct feeding, is used for preventing and treating common clinical cattle diseases, achieves disease prevention and treatment and health invigoration effects, has the advantages of good palatability, autonomous feeding, convenience in use and the like, and solves the problems of operation time and energy waste, animal stress reaction, pain and the like caused by drenching and injection administration. In addition, the drug carrier is simple in production technology, extensive in raw material source and low in production cost, and is suitable for large-scale production.
CA2659055A1 2-phenyl-indoles as prostaglandin d2 receptor antagonists The present invention is directed to 2-phenyl-indole compounds (A), their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, eczema, urticaria diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.
US8673586 Compounds that interact with kinases A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide, or a pharmaceutically acceptable salt thereof.
US6858235 Antioxidant composition and method of preparation thereof The present invention relates to an antioxidant composition and a method of preparation thereof. In detail, the present invention relates to an antioxidant composition containing procyanidin B3 obtained from Rosa multiflora, and a preparation method for the antioxidant composition, comprising extraction of the underground part of Rosa multiflora with an organic solvent, followed by fractionation and purification of the extract by chromatography. The antioxidant composition of the present invention can be effectively used in treatment or prevention of various diseases due to oxidation by reactive oxygen species, maintenance of quality of food, and prevention of skin damages due to oxidation.
US20080015174 Metabolic Disease Treatments The invention relates to the use of compounds to treat a number of conditions, such as a pre-diabetes condition, type 1 diabetes, type 2 diabetes, hyperglycemia, insulin resistance and glucose intolerance. Compounds that can be used in one or more of the treatment methods include 3β,7β,16α,17β-tetrahydroxyandrost-5-ene, 3α,7β,16α,17β-tetrahydroxyandrost-5-ene, 3β,7β,16α,17β-tetrahydroxyandrost-5-ene, 3β,16α,17β-trihydroxyandrost-5-ene-7-one, 3β,7β,17β-trihydroxy-17α-ethynylandrost-5-ene, 3β,17β-dihydroxy-17α-ethynylandrost-5-ene-7-one and 3β,7α,17β-trihydroxy-17α-ethynylandrost-5-ene.
WO2010033045A1 Compositions and methods for prevention or treatment of beta amyloid deposition The present invention relates to methods of preventing or treating amyloid beta protein deposition in a mammal in need thereof comprising administering to said mammal an effective amount of succinic acid or a pharmaceutically acceptable salt thereof. Further, invention relates to the use of succinic acid or a pharmaceutically acceptable salt thereof for manufacturing a pharmaceutical composition for preventing or treating amyloid beta protein deposition in a mammal in need thereof. Further, pharmaceutical composition for preventing or treating amyloid beta protein deposition in a mammal in need thereof comprising (a) succinic acid or a pharmaceutically acceptable salt thereof and (b) a pharmaceutically acceptable carrier. Preferably, the mammal is a human. Preferably, the amyloid beta protein deposition is associated with Alzheimer's disease, Down's syndrome, glaucoma, and age-related macular degeneration (AMD).
US20050171062 Administering to an animal having ocular hypertension or inflammatory bowel disease a piperidynly analog as for example 7-[2-oxo-6-((E)-3-oxo-oct-1-enyl)-piperidin-1-yl]-hept-5-ynoic acid methyl ester The present invention provides a method of treating inflammatory bowel disease which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula 1; wherein X, Y, Z, D and R3 are as defined in the specification. Also useful for the treatment of inflammatory bowel disease are compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein A, X, J, and R3 are as defined in the specification. Also useful for the treatment of inflammatory bowel disease are compounds having an α and an ω chain comprising or derivatives thereof, as defined in the specification or pharmaceutically acceptable salts or prodrugs thereof.
WO2014025905A1 Multi-component formulation for improving neurological function In certain embodiments multi-component formulations are provided where the formulations comprise a first component comprising one or more vitamins selected from the group consisting of one or more B vitamins, vitamin C, vitamin D, vitamin E, co-enzyme Q10, vitamin K, and folate; a second component comprising one or more elements selected from the group consisting of selenium, lithium, magnesium, and molybdenum; a third component comprising one or more omega-3 fatty acids; and a fourth component comprising one or more amino acids selected from the group consisting of trimethylglycine, N-acetyl cysteine, S-adenosyl methionine, L-tryptophan, and glutathione.
EP2783690A1 New use of neohesperidin The present invention discloses a use of neohesperidin or a neohesperidin-containing plant extract in the manufacture of a product for improving and/or promoting skin microcirculation, or for eliminating and/or alleviating diseases or conditions associated with poor skin microcirculation. The present invention also discloses a composition comprising an effective amount of neohesperidin or a neohesperidin-containing plant extract, and to a method for improving and/or promoting skin microcirculation, or eliminating and/or alleviating diseases or conditions associated with poor skin microcirculation, by using neohesperidin. The skin microcirculation of the present invention is preferably eye skin microcirculation.
WO2014163643A1 Gga and gga derivatives compositions thereof and methods for treating neurodegenerative diseases including paralysis including them This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.
US7470719 Metastable benzoxepne derivatives which can be used in the treatment of dyslipidaemia a therosclerosis and diabetes, pharmaceutical compositions comprising them and processes for the preparation thereof The present invention relates to novel metastable derivatives of benzoxepines of the formula (I) in which n represents 0, 1 or 2; and the radicals R, which may be identical or different, are alkyl or alkoxy groups, or halogen atoms, which can be used in the treatment of dyslipidaemia, atherosclerosis and diabetes.
WO2010150819A1 Therapeutic agent for ischemic cerebrovascular disorders A therapeutic agent for ischemic cerebrovascular disorders, which comprises a substance capable of inhibiting the function of interleukin 17, interleukin 23 or γδT cells or the invasion of γδT cells into the brain.
CN103751030A Application and preparation method of Beauveria sp extract having tyrosinase inhibition activity The invention relates to an application and a preparation method of a Beauveria sp extract having tyrosinase inhibition activity, specifically to an application of the Beauveria sp extract in preparation of pigmentation and melanoma prevention and treatment tyrosinase inhibitors. According to the present invention, the main effective component in the Beauveria sp extract is 6'-methyl-2',4'-dihydroxyphenyl-4-O-methyl-beta-D-glucopyranoside, and the content is 5-99%; the activity is characterized in that the half-inhibition concentration (IC50) on the tyrosinase is 37.6-638.5 mug/mL; and the Beauveria sp extract having the tyrosinase inhibitor has wide uses, can be adopted as the daily chemical additive, and provides effects of whitening, anti-blackening, anti-aging, pigmentation and melanoma prevention and treatment, and the like.
CN1634072A Levofloxacin dripping pills and its preparing process The invention discloses a lactic acid levofloxacin dripping pills and its preparing process, wherein each drop pill contains Levofloxacin 1-10 mg and right amount of drop pill base material, the drop pill base material is selected from one or two of polyethylene glycol 6000, polyethylene glycol 4000, polyoxyethglene monostearate, sodium stearate, glycerol gelatine, poloxamer, stearic acid, glyceryl monostearate, insect wax. And the preparing process comprises the steps of heating till melting, mixing homogeneously, instilling into condensation agent, taking-up and removing the condensation agent, checking and packaging.
US7884080 Administering an azetidinone compound for treating a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease; T-type calcium channel blocking agent, an antagonist of TRPV1, an agonist of TRPV1, of GPR119, antagonist of NPCL1 The present invention relates to Azetidinone Derivatives of structural formula 1: and compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.
US20110123483 Hmgb1 for cancer treatment The current invention relates to a method for treating a subject suffering from cancer comprising administering to said subject a therapeutically effective dose of High Mobility Group B1 (HMGB1) protein or of a polynucleotide comprising a coding region for an HMGB1 gene in an expressible form. Moreover, it relates to the combination of said method with other cancer treatment regimens.
CN102657665A Compound dehydration and diuresis medicine composition The invention relates to a compound dehydration and diuresis medicine composition, which contains mannitol, piracetam, 1,6-fructose diphosphate, pharmacological acceptable carriers, glucose and hydrogen chloride thiazole. The compound dehydration and diuresis medicine composition uses mannitol, piracetam and 1,6-fructose diphosphate as the main components, is fast in dosing and long in lasting time and can remarkably reduce using amount of mannitol and piracetam through synergistic effects simultaneously, so that side effects caused by mannitol and piracetam can be remarkably reduced, and thecompound dehydration and diuresis medicine composition is suitable for prevention and treatment of intracranial hypertension.
WO2013138602A1 An iloperidone metabolite for use in the treatment of psychiatric disorders R-P88 is used for the treatment of disorders amenable to treatment with an atypical antipsychotic.
WO2011159781A2 Bitter taste modulators The present invention includes antagonists of human type 2 taste receptors (hT2Rs) having structural Formula (I). The present invention also provides compositions containing these antagonists, the use of these antagonists for modulating taste perception, particularly bitter taste, and the method of preparing these antagonists (I).
CA2259936C Apoptosis inducing adamantyl derivatives and their usage as anti-cancer agents The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen--independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.
WO2010134827A9 Extended acting oxygen generating composition for treating microbial infections A medicament for the treatment or prevention of a microbial infection or an associated condition in a low oxygen environment characterised in that the medicament includes an extended acting oxygen generating system.
WO2008058537A1 Novel 2-amino-pyridine derivatives and their use as potassium channel modulators This invention relates to novel 2-amino-pyridine derivative useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
CN102600186A Application of cyclophosphamide compound in preparing information treatment drug, preparation method and prepared novel drug The invention discloses application of a cyclophosphamide compound in preparing an information treatment drug, a preparation method of the cyclophosphamide compound and a novel drug prepared by the preparation method. During the treatment, the information treatment drug does not directly touch a human body, drug substance components are not consumed, chemotherapy effects can be achieved only by drug information physiotherapy, and the therapy window is enlarged more than one thousand times, and side effects of the chemotherapy are avoided. After cyclophosphamide is used as the information treatment drug, the effective component content is not changed, and cyclophosphamide can also be used secondarily and effectively as a chemotherapy normal preparation.
WO2008142859A1 Novel spiro-oxindole compound and pharmaceutical containing the same A spiro-oxindole compound represented by the formula (I) a salt thereof or a solvate thereof of the invention exhibits an excellent inhibitory effect on 11β-hydroxysteroid dehydrogenase type 1, and is useful as a preventive or therapeutic agent for a disease associated with 11β-hydroxysteroid dehydrogenase type 1 (particularly diabetes, insulin resistance, diabetic complication, obesity, hyperlipidemia, hypertension, fatty liver or metabolic syndrome). (I)
WO2009095923A3 Corroles for neuroprotection and neurorescue Transition metal complexes of amphiphilic corroles, optical isomers and pharmaceutically acceptable salts thereof are useful for neuroprotection and neurorescue, particularly for treatment of diabetes and neurodegenerative diseases. The amphiphilic corrole is preferably a 5,10,15-tris-aryl- or 5,10,15- tris-CF3-corrole, and said transition metal complex more preferably has the formula I defined in the specification. Also provided are propargyl-containing corroles carrying one or more radicals substituted by a propargylamino group or one or more nitrogen-containing heteroaryl radicals substituted by propargyl at the ring N atom.
CN102119934B Application of verbascoside in preparation of medicaments for treating chronic prostatitis The invention discloses new application of verbascoside, in particular application of the verbascoside in the preparation of medicaments for treating chronic prostatitis and application of the verbascoside serving as an active ingredient in the preparation of compound preparations. Researches show that the verbascoside has an obvious suppressing effect on chronic prostatitis model rats, and the treating effect is better than that of Prostate Plus.
EP1499619A1 Bicyclic heterocycles, medicaments containing these compounds, their use, and method for the production thereof The invention relates to bicyclic heterocycles of general formula (I), in which Ra, Rb, Rc, A, B, C, D, E and X are defined as in Claim 1, to tautomers, stereoisomers, mixtures and salts thereof, particularly their physiologically compatible salts with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory action on the signal transduction imparted by tyrosine kinases. The invention also relates to the use of these compounds for treating diseases, particularly tumor diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and of the respiratory passages and to the production thereof.
US7276604 Stable in humid environments; bone resorption disorders; mixing and heating an aqueous solution of the salt hydrate with isopropanol and crystallizing during slow cooling The present invention relates to a crystalline, hydrated form of the sodium salt of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid. The hydrate contains from 6.4 up to 22 weight % of sodium and 15 up to 23 weight % of crystalline water if the sodium content is lower than 7.5 weight %, based on the whole molecule, or 4.5 up to 18 weight % of crystalline water if the sodium content is equal to or higher than 13 weight %, based on the anhydrous substance. Due to stability in humid environments, the hydrate is useful as an active substance for the treatment of diseases associated with bone resorption disorders.
US20080031939 Process for the preparation of armodafinil The invention encompasses processes for preparing intermediates, such as R-modafinic acid or (R)-C1-2 alkyl ester, of modafinic acid, and the conversion of the intermediates to armodafinil.
US20120040930 Tetracyclic terpene series compounds, methods for preparing same, uses thereof as medicines and pharmaceutical compounds containing same The invention concerns a triterpene alkaloid of general formula (I). The invention also concerns a method for making same and use thereof as medicine.
EP1838324A2 Novel farnesyl protein transferase inhibitors and their use to treat cancer Disclosed are compounds of the formula: wherein R8 represents a cyclic and acyclic moiety to which is bound an imidazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
US20100272827 Method for transdermal iontophoretic delivery of chelated agents Embodiments provide devices, systems and methods for the transdermal delivery of chelated compounds. One embodiment provides a method for the iontophoretic transdermal delivery of a chelated iron complex for the treatment of anemia. A first patch comprising an active electrode and a chelated iron complex is applied to the skin; a second patch containing an electrode is also applied. An electrical current is then delivered to the skin from the active electrode. The chelated complex is transported across the skin via electromotive force from the current, with the iron being substantially chromogenically unreactive with the skin during transport so that there is little or no tattooing of the skin due to the formation of insoluble oxidative products. The complex is then dissociated by phagocytosis or related process to release the iron where it may be bound by transferrin or ferritin and carried to other sites for storage or metabolic use.
US7812015 Using tricyclic or tetracyclic antidepressant amitryptiline, imipramine, desipramine or FGF as inhibitors of acid sphingomyelinase which liberates ceramide, for prophylaxis and/or treatment of infectious diseases ( AIDS, hepatitis A, tuberculosis, rubella, SSME, influenza, rhinoviral diseases, malaria) The invention relates to the use of inhibitors of acid sphingomyelinase and/or of inhibitors of products of the reaction catalyzed by this enzyme, for the prophylaxis and/or treatment of infectious diseases and/or diseases which are influenced by infections during the course thereof. The cited products especially include ceramide. Preferrably neutralizing antibodies and/or antidepressants, especially tricyclic and/or tetracyclic antidepressants, are used as inhibitors.
CN101785755A Antofloxacin hydrochlorid injection and preparation method and purpose thereof The invention relates to an antofloxacin hydrochlorid injection containing antofloxacin hydrochlorid salt, an isotonic agent and water for injection, which is characterized in that each 100 milliliters of antofloxacin hydrochlorid injection contain 0.1 g-2 g of antofloxacin hydrochlorid. The invention also provides a preparation method of the antofloxacin hydrochlorid injection, which is characterized in that the content of an intermediate is controlled to 98.0%-101.0% of the labeled amount, and the pH value of a buffer is controlled to 5.2-5.3. The antofloxacin hydrochlorid injection is mainly used for preventing and treating the bacterial infection of people or animals. The injection can be administrated in veins and arteries, under skin and in muscles and peritoneum, wherein intravenous administration is the most important administration approach, the suitable dosage is that 200mg of antofloxacin hydrochlorid is injected each time and is intravenously injected once every day. In generally, the concentration of the used antofloxacin hydrochlorid is 0.1% (w/v), equivalent to 100 mg/100ml.
CN1720930A Anti-AIDS material drug, tablet, capsule, oral liquid and preparation method thereof The invention relates to the raw material medicament, tablet, capsule and oral liquid of antiretroviral medicament with appreciable effect for treating AIDS, whose preparing process consists of cantharis selection, disintegrating, cantharidin extraction, cantharidin degreasing, methylcantharidinimide synthesizing, methylcantharidinimide refining, a series of technical procedures of formulation combination, tabletting, loading, and packaging.
CN101993424A Lariciresinol and derivative, preparation method and application thereof The invention discloses lariciresinol and a derivative, a preparation method and application thereof. The lariciresinol is a lignin compound with benzene ring and tetrahydrofuran ring, and the derivative is ester of the lignin compound and monosaccharide or polysaccharide; in the general formula of the molecular structure, R1 represents hydroxyl and ester of hydroxyl and monosaccharide or polysaccharide. In the invention, the preparation method adopts multistage extraction and resin establishment; the lariciresinol is prepared by the steps of: extracting lariciresinol-di-glucopyranoside in radix isatidis, re-crystallizing the lariciresinol-di-glucopyranoside, and carrying out hydrolysis in an acidic condition; and the derivative of the lariciresinol is prepared by a step of carrying out derivatization reaction on the re-crystallized lariciresinol and the monosaccharide or polysaccharide in the presence of dichloromethane and dicyclohexylcarbodiimide.
WO2011136634A1 Preventing salmonella infection induced weight loss A method involving administering pectin degradation product is provided for preventing and/or treating weight reduction in subjects suffering from salmonella infection or susceptible to salmonella in infection.
CN101357124A Medicine for treating osteoarthritis The invention discloses a medicine which cures osteoarthritis and is a compound which is formed by combining (S)-ibuprofen and dextrosamine or the medicine salt thereof according to 1:3 of mass ratio. The (S)-ibuprofen and the dextrosamine are prepared into compound preparation. The characteristics of rapid drug effects and strong abirritation of the (S)-ibuprofen can be used for rapidly relieving symptoms on the one hand; on the other hand, the dextrosamine can defer cartilage degeneration process, repairs cartilage pathological changes, and prevents, even reverses the disease process. Meanwhile, the (S)-ibuprofen and the dextrosamine are prepared into the compound preparation, which can reduce the dose of single medicine and further reduce the toxic side effects. The compound preparation prepared by the (S)-ibuprofen and the dextrosamine of the invention becomes a new medicine which can cure the osteoarthritis.
US20100234469 New Crystals Of A Benzoylbenzeneacetamide Derivative The invention relates to 2-amino-3-benzoylbenzeneacetamide, i.e. nepafenac, crystals having reduced chargeability, to processes for the preparation thereof, and to the use thereof for preparing pharmaceutical formulations.
CA2259781C Low tack lotion, gels and creams The present invention relates to a mixture of a silicone wax,a silicone fluid and two long chain lactate molecules which is effective in reducing the tacky feel of compositions. The present invention is suitable for use in creams, gels, lotions and salves that are applied to the skin.
WO2007134451A1 Oligonucleotides affecting expression of phosphodiesterases The invention relates to therapeutic antisense oligonucleotides directed against genes encoding phosphodiesterases (PDE) and the use of these antisense oligonucleotides in combination. These antisense oligonucleotides may be used as analytical tools and/or as therapeutic agents in the treatment of disease associated with reduced cellular cAMP in a patient, such as inflammatory diseases of the respiratory tract including, for example, asthma, chronic obstructive pulmonary disease (COPD), acute respiratory distress syndrome, bronchitis, chronic bronchitis, silicosis, pulmonary fibrosis, lung allograft rejection, allergic rhinitis and chronic sinusitis as well as other conditions in which an increase in cyclic AMP or a decrease in PDE levels is beneficial.
EP1973894A2 Method for preparation of amorphous, anhydrous crystalline, or hydrated crystalline docetaxel This invention is directed to a method for the preparation of docetaxel having an amorphous, anhydrous crystalline, or hydrated crystalline structure. In accordance with the invention, highly pure amorphous, anhydrous crystalline, or hydrated crystalline docetaxel can be produced with a high yield by using a solvent precipitation method, colloid formation method, etc.
US20050085860 Transdermal/transmucosal preparations for electroporation A preparation for transdermal or transmucosal administration for electroporation is provided that enables efficient administration of a compound to be administered such as a drug. The preparation for transdermal or transmucosal administration for electroporation includes a drug reservoir (11) having dispersed therein a compound to be administered (physiologically active substance), such as a drug, in a base of a solid or semisolid form, a backing (12) retaining the drug reservoir, and a pair of electrodes for electroporation (13) provided on the drug reservoir (11). An adhesive layer (14) is provided on a flange portion of the backing (12). An insulating layer (15) is provided on at least a section of the electrodes for electroporation (13) contacting an application site other than a section on the drug reservoir (11).
US7374931 Vaccine against staphylococcus intoxication Using nucleic acids encoding mutant SEA and SEB exotoxins from Staphylococcus aureus, compositions and methods for use in inducing an immune response which is protective against staphylococcal aureus intoxication in subjects is described.
US20050043413 Active ingredient for producing a substance containing isocitrate for influencing the coagulation tendency of blood An active ingredient for producing a medicament for inhibiting the coagulation of blood, and a corresponding medicament are provided. The active ingredient is isocitrate or an active derivative thereof.
US20080076753 Substituted spiroheterocycles The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal insufficiency, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.
US20080312204 Soluble forms of amoxicillin and treatment of animals A solid mixture or aqueous solution of amoxicillin antibacterial agent with a material that aids in its dissolution in water to render it ingestive and palatable.
US20130309173 Methods and compositions for maintenance of a functional wound The present invention relates to methods and compositions for the modulation of wound healing and/or the production of extracellular membrane components by modulating the activity and/or amount of secreted protein acidic and rich in cysteine (SPARC) protein. The invention further provides methods for identifying compounds useful in the above-mentioned methods and compositions.
WO2009075277A1 4-aminopyrimidine derivative and medicinal composition containing the compound A compound represented by the following general formula (I) [wherein R1 represents halogeno or a group, or R1 represents the following formula (II): (wherein R5 represents C6-10 aryl optionally substituted with one or more halogen atoms or represents another group); and one of R2 and R3 is hydrogen and the other represents -(CH2)nR4 (wherein n is 0, 1, 2, or 3 and R4 represents hydrogen, hydroxy, or another group), or R2 and R3 in combination may form an optionally substituted 4- to 8-membered heterocyclic group in cooperation with the adjacent nitrogen atom]; a pharmacologically acceptable salt of the compound; or a hydrate or solvate of either.
CN102028657A Solid preparation of acetylcysteine liposome The invention discloses a solid preparation of acetylcysteine liposome, which is mainly prepared from acetylcysteine, phospholipid and an additive with the weight ratio of 1:1-9:0.3-5. Furthermore, the solid preparation of acetylcysteine liposome is prepared into a pharmaceutically acceptable solid preparation, thus, on one hand, the lipid solubility and the bioavailability of the solid preparation can be increased, and on the other hand, the solid preparation plays a protection role in drugs, increases the stability of the drugs, improves the product quality and reduces the toxic or side effect.
WO2006101108A1 Novel cyclic aminophenylalkanoic acid derivative [PROBLEMS] To provide a cyclic aminophenylalkanoic acid derivative which can act as a human peroxisome proliferator activated receptor (PPAR) agonist, particularly an agonist of a human PPARα isoform and is effective for the treatment of a disorder of lipid metabolism, diabetes or the like or an addition salt thereof, and a pharmaceutical composition comprising the derivative or salt. [MEANS FOR SOLVING PROBLEMS] A cyclic aminophenylalkanoic acid derivative represented by the general formula (1) or a pharmacologically acceptable salt thereof.
CN103566035A Medicament for treating non-ruptured chilblain The invention discloses a medicament for treating non-ruptured chilblain. The medicament is characterized by comprising the following components: 3-7g of carbolic acid, 3-7g of camphor, 3-7g of menthol, 3-7g of resorcinol, 3-7g of boric acid, 2-8g of lanum, 2-8g of vaseline, 6-12g of eggplant stalk, 6-12g of chili stalk, 6-12g of Chinese waxgourd peel, 6-12g of cinnamon, and 6-12g of white radish. The medicament can remarkably improve and relieve signs and symptoms of local stasis swelling and pains of non-ruptured chilblain, and is unique in cure rate and low in relapse rate, the cure rate is over 70 percent, and the total effective rate is over 90 percent.
EP1107722B1 A method for the treatment of staphylococcal infection Lysostaphin is an effective antibiotic in the treatment of staphylococcal infection. Large doses of lysostaphin or lysostaphin analogues are effective in short course, or even one dose administration, in treating and eradicating staphylococcal infections, including those resistant to conventional antibiotics.
CA2191747C (a)-annelated pyrrole derivatives and pharmaceutical use thereof The present invention relates to heterocyclic compounds of the formula (see formula I) in which R1-R7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid variety and for the prevention of allergically induced diseases.
CN102440965A Esomeprazole sodium composition used for injection and its preparation method The invention provides an Esomeprazole sodium composition used for injection and its preparation method, the Esomeprazole sodium composition is prepared by the following steps: 1) liquid preparation: selecting esomeprazole sodium and ethylenediamine tetraacetic acid or ethylenediamine tetraacetic acid salt as raw materials, wherein the weight ratio of esomeprazole sodium to ethylenediamine tetraacetic acid or ethylenediamine tetraacetic acid salt is 1:0.01-0.1, weighting a proper amount of raw materials into a preparation tank, and adding water for injection to the weight of 23.47-234.7 timesof esomeprazole sodium, stirring and uniformly mixing the solution, adjusting the pH value of 10.0-12.5; 2) activated carbon finishing; 3) adsorbing; 4) sterile filtrating and split charging; 5) vacuum freeze-drying to obtain the esomeprazole sodium composition used for injection. The esomeprazole sodium composition used for injection and the preparation method are capable of ensuring the heat source, visible foreign matter and insoluble particulate to accord with the requirements of the injection for the injection preparations such as esomeprazole sodium preparation liquid with high pH value.
US20100074951 Controlled release complex composition comprising angiotensin-ii-receptor blockers and hmg-coa reductase inhibitors Disclosed herein is a lag time delayed-release combination pharmaceutical composition comprising of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor, as well as a preparation method thereof. The composition is designed based on chronotherapy in which active ingredients are administered to have different onset times, such that the release of each active ingredient of the composition in body can be lag time delayed to a specific rate. Also, the composition is very effective for the treatment of hypertension and the prevention of complications in patients having metabolic syndromes which show diabetes, obesity, hyperlipidemia, coronary artery diseases and the like. More specifically, the composition is a drug delivery system designed such that the release of each drug is controlled to a specific rate, and it can show the most ideal effect, when it is absorbed in body.
US6958344 Pyrimidine compounds and their use as modulators of chemokine receptor activity The invention provides certain heterocyclic compounds, processes, and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy; in formula (I), A is a group of formula (a) or (b).
US20120164080 Methods of treatment for esophageal inflammation Provided herein are methods for treating gastrointestinal inflammation, for example, esophageal inflammation, or reduction of eosinophilic infiltration of the esophagus and/or reducing local and systemic exposure and/or side effects resulting therefrom. Provided herein are methods for diagnosing gastrointestinal inflammation, for example, esophageal inflammation, or reduction of eosinophilic infiltration of the esophagus. Also provided herein are methods for inducing remission of eosinophilic infiltration of the esophagus
CN101912491B Pills for treating cardiovascular diseases and preparation method The invention relates to pills for treating cardiovascular diseases, which are prepared from natural plants serving as a main pharmaceutic component and specific pharmaceutic adjuvants. The pills are prepared from the following raw materials and adjuvants in part by weight: 18 parts of parslane herb, 18 parts of obscured homalomena rhizome, 18 parts of szechuan lovage rhizome, 18 parts of root ofred-rooted salvia, 20 parts of rosewood heart wood, 8 parts of borneol, 8 to 12 parts of PEG 4000 and 67 to 73 parts of PEG 6000. The specific pharmaceutic adjuvants are added in the pills, so that the medicament is in a highly dispersed state or molecular dispersion state in a matrix to prevent the aggregation of molecular crystals and improve the stability of the medicament, and ferulic acid serving as an active substance in the medicament is kept stable to prevent the ferulic acid from being decomposed or converted and enhance the effects of antioxidation, thrombus resistance and blood fatreduction of the medicament; simultaneously, the pills can increase or improve the dissolvability of the medicament obviously, accelerate the dissolution or absorption of the medicament, bring the pharmacological effect of the medicament into play quickly and have the quick-acting effect on symptoms which needs to be relieved quickly, and the effect of the pills is superior to that of congeneric products.
EP1685105B1 Allosteric modulators of metabotropic glutamate receptors The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, Rl and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
US6995171 Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents The invention relates to compounds of the formulas 1 and 2 and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein X, R1 and R11 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1 and 2 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formulas 1 and 2.
EP2540292A1 DHA and EPA in the reduction of oxidative stress The present invention generally relates to the prevention or treatment of disorders related to oxidative stress. For example, the present invention provides a composition for use in the prevention or treatment of oxidative stress related disorders under post-operative conditions. One embodiment of the present invention is a composition comprising DHA and EPA as active ingredients for use in the treatment or prevention of oxidative stress and/or related disorders.
WO2006109729A1 Pyridylmethylsulfone derivative Disclosed is a novel compound having an effect of inhibiting the production/secretion of β-amyloid protein. A compound represented by the general formula (1) or a salt or a solvate of the compound or the salt; and a pharmaceutical agent comprising the compound, salt or solvate.
CN1882698B Hypoxia-inducible protein 2 (HIG2)serving as a novel therapeutic potential target of renal cell carcinoma (RCC) The present invention provides a method for inhibiting growth of a cancer cell, particularly a renal cell carcinoma, by contacting the cell with a composition composed of an HIG2 siRNA or HIG2 antibody. Methods of diagnosing renal cell cancer are also provided within the present invention.
CN101259108A Double-unit tablet containing acid-labile medicaments The invention describes an oral solid preparation of labile active ingredient of acid which comprises two laminas that are disintegrated according to priority, wherein the lamina A comprises a highly effective disintegrant and a basifier, so the disintegrating speed is quicker, the lamina A can quickly release the basifier in gastric juice, and in virtue of which the pH value of the gastric juice is raised; the labile active ingredient of acid of the lamina B is dispersed in the material of a carrier with retarding action to ensure the release of the active ingredient a certain time of lag. A double-unit tablet provided by the invention has simple preparation technique and good stability in storage, which is especially applicable to drugs of labile acid such as proton pump inhibitor.
US7358333 Polypeptides of the IFNα-5 gene The present invention relates to new polynucleotides derived from the nucleotide sequence of the IFNα-5 gene comprising new SNPs, and new polypeptides derived from the natural wild-type IFNα-5 protein comprising at least one mutation caused by at least one SNP of the invention as well as their therapeutic uses.
US20080305171 Pyrrolopyrazine, formulations, methods of manufacture, and methods of use there Disclosed herein is a pyrrolopyrazine COMPOUND I having defined amounts of R isomer, particle size, and stability. Also disclosed are pyrrolopyrazine oral dosage forms comprising the described COMPOUND I material as well as methods of treating disorders amenable to therapy using COMPOUND I.
WO2008156160A1 Composition for transdermal or transmucosal administration [PROBLEMS] To provide a composition for transdermal or transmucosal administration which is useful as an anti-Alzheimer's disease drug, an anti-Parkinson's disease drug, an antidepressant drug, a psychotropic drug, a remedy for drug dependence or the like. [MEANS FOR SOLVING PROBLEMS] A composition for transdermal or transmucosal administration, which contains an effective amount of a racemic body or optically active isomer of 1-(benzofuran-2-yl)-2-propylaminopentane or its pharmacologically acceptable salt and a vehicle and can be administered without invading the skin or mucosa, is excellent as an anti-Alzheimer's disease drug, an anti-Parkinson's disease drug, an antidepressant drug, a psychotropic drug or a remedy for drug dependence, since the composition enables the stable accession of an effective amount of the active ingredient into the body or brain via the skin or mucosa without causing any trouble such as a loss in the active ingredient due to the first pass effect in the liver, a pain, an injury or infection.
CN101590017A Method for preparing taxol magnetic nano liposome Taxol is a great discovery in the field of antineoplastic medicaments within recent 20 years, has high lipotropy and can not be dissolved in water. The prior dosage forms in the markets are of injection type, using polyhydroxy ethyl castor oil and ethanol as a solvent, wherein the ratio of the polyhydroxy ethyl castor oil and the ethanol is 1:1; before using, the solvent is diluted to 0.3-1.2 mg/ml by dextran, and the like. The toxic side effects of the solvent and the taxol obstruct the clinical application. At present, the taxol has no targeted preparation with better targeted effects. The invention aims to provide a taxol magnetic nano liposome targeted preparation. The method for preparing the magnetic liposome adopts a microemulsion-low temperature curing method, comprising the following steps: mixing oil phase (stearic acid), a surfactant (Tween-80) and cosurfactant (ethanol) in water bath with the temperature of 73 +/-2 DEG C, dripping a certain amount of distilled water to form a transparent system, adding dispersed magnetic liquid rapidly, stirring uniformly to form suspension containing magnetism, injecting the mixed suspension to the water in an ice bath to disperse, obtaining product particle suspension, dialyzing and rinsing the suspension, freezing and drying to obtain the magnetic solid liposome nano particles.
US20080318911 20-Cyclopropyl, 26,27-Alkyl/Haloalkyl Vitamin D3 Compounds and Methods of Use Thereof The invention provides vitamin D3 analogs of cholecalciferol, substituted at carbon 20 with cycloalkyl, e.g., cyclopropyl, wherein carbon-16 is a double bond, and carbon-23 is a single, double, or triple bond. Various alkyl or haloalkyl substitutions are incorporated as carbon-25. The invention provides pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.
WO2014013076A1 Hexahydropyrrolothiazine compounds A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R9 are as defined in the specification and which compound has an Αβ production inhibitory effect and may be useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Αβ and typified by Alzheimer-type dementia (AD) or Down's syndrome.
CN101843850A Medicinal liquor for treating male reproductive hypofunction and preparation method thereof The invention relates to medicinal liquor for treating male reproductive hypofunction, which is prepared from the following components in part by weight: 30 to 50 parts of whole Chinese angelica, 30 to 50 parts of Indian bread with hostwood, 30 to 50 parts of medicinal cyathula root, 30 to 50 parts of eucommia bark(stir-fried with vinegar and sliced), 30 to 50 parts of walnut kernel (peeled), 30 to 50 parts of raisin (peeled), 30 to 50 parts of medlar, 30 to 50 parts of longan pulp, 10 to 20 parts of clove, 10 to 20 parts of elecampane inula root, 10 to 20 parts of actinolite, 10 to 20 parts of flower of silktree albizzia, 10 to 20 parts of spina date seed, 10 to 20 parts of dendrobium, 10 to 30 parts of ginseng and 600 to 800 parts of Yantai Changyu sanbian wine. The medicinal liquor prepared by a method for strictly controlling preparation process and preparation season has good effects of treating the male reproductive hypofunction and male hypogonadism.
CN102234275A Deuterated imidazo [1, 2-a] pyridine derivative for treating insomnia, its preparation method and applications The invention relates to a compound as the formula 7 or pharmaceutically acceptable salt, wherein, R1, R2, R3, R4 and R5 represent H (hydrogen) or D (deuterium), and at least one of the R1-R5 represents D. The invention also relates to the preparation method of the compound, a medicinal composition comprising the compound as active component, and the applications of the compound or pharmaceutically acceptable salt in preparing the medicines for treating insomnia, inducing sleep and keeping sleep.
EP1951245A2 Pharmaceutical compositions comprising methotrexate The present invention relates to pharmaceutical compositions and their uses in therapy. In particular, the invention relates to compositions comprising methotrexate, preferably wherein the compositions are for administration via the inhaled or intranasal route.
US20090137647 Modified Macrophage Migration Inhibitory Factor Inhibitors Provided are various compounds of Formula I (I). Also provided are various compounds of Formula II (II). Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also providcd are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.
US20110224274 New Therapeutic Agents A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.
US20130005666 Reporter system for high throughput screening of compounds and uses thereof The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2 we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). It is shown herein that Neh2 domain is sufficient for recognition, ubiquitination and proteasomal degradation of Neh2-luciferase fusion protein. The novel Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time-course of reporter activation. The novel reporter was used to screen a library of compounds to identify activators of Nrf2. The most robust and yet non toxic Nrf2 activators found—nordihydroguaiaretic acid, fisetin, and gedunin-induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism.
US20120165377 Agent for reducing visceral fat weight An FGF21 production promoting agent containing, as an active ingredient, a compound represented by the following formula (1): wherein each of R1 and R2, which may be identical to or different from each other, represents, for example, a hydrogen atom; each of R3a, R3b, R4a, and R4b, which may be identical to or different from one another, represents, for example, a hydrogen atom or a halogen atom, or R3a and R3b or R4a and R4b may bond together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents, for example, a hydrogen atom or a C1-4 alkyl group); Y represents, for example, an oxygen atom, an S(O)l group (l is a number of from 0 to 2), or a carbonyl group; Z represents CH or N; n is a number of from 1 to 6; and m is a number from 2 to 6, a salt of the compound, or a solvate of the compound or the salt.
WO2011052759A1 Novel nitroxyl radical compound and process for production thereof Disclosed are: a process for producing a novel nitroxyl radical; and the compound. The nitroxyl radical produced by the process has a therapeutic effect on gastric ulcer and hypertension.
US20120100182 Continuous Cell Programming Devices The present invention comprises compositions, methods and devices for creating an infection-mimicking environment within a polymer scaffold to stimulate antigen-specific dendritic cell activation. Devices of the present invention are used to provide protective immunity to subjects against infection and cancer.
WO2013123165A1 Crystalline form of (2s,4r)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(1h-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid [1,3]dioxol-4-ylmethyl ester The invention provides a crystalline form of (2S,4R)-5-biphenyl-4- yl-2-hydroxymethyl-2-methyl-4-[(lH-[l,2,3]triazole-4-carbonyl) amino]pentanoic acid 5-methyl-2-oxo-[l,3]dioxol-4-ylmethyl ester or its tautomer. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.
CN102793706A Preparation method of tolvaptan solid dispersion The invention provides a preparation method of a tolvaptan solid dispersion. The method adopts hot melting and extrusion technology; in particular, tolvaptan, carriers, and a plasticizer are mixed, heated, melted, and cooled to obtain the solid dispersion. The method of the invention has the characteristics of high efficiency and simple production process, and the solid dispersion prepared by the method of the invention has good dissolvability.
CN203329063U Disintegration-structure DHA (docosahexenoic acid) soft capsule The utility model relates to a disintegration-structure DHA (docosahexenoic acid) soft capsule which comprises a content containing DHA and a capsule shell filled with the content, wherein at least one quick disintegration area is formed on the surface of the capsule shell; multiple grooves are formed in the inner surface of the quick disintegration area; generally, the quick disintegration area occupies 1/5-4/5 of the surface area of the whole capsule shell. The disintegration-structure DHA soft capsule provided by the utility model has the beneficial effects that the disintegration-structure DHA soft capsule is quickly disintegrated and not easily aged, the storage life can be prolonged, and the curative effect is stable. Through observation under high temperature, high humidity, illumination and the like, the excellent rate can be kept 11% higher than that of a common soft capsule, and the average disintegration time of multiple batches is about 20-30 minutes.
CN101991567A Application of three biflavone monomer components extracted from ginkgo leaves in preparing medicament of alpha-glucosidase inhibitor The invention provides three biflavone compounds, namely ginkgetin, isoginkgetin and 7-bilobetin from dry leaves of ginkgo biloba L. Pharmacological tests prove that the three biflavone compounds have the activity of inhibiting alpha-glucosidase. The invention discloses novel application of the ginkgetin, the isoginkgetin and the 7-bilobetin in preparing the alpha-glucosidase inhibitor, and also discloses a novel method for preparing the three biflavone compounds.
WO2010079514A1 A process for preparation of hexadecyl cis-9-tetradecenoate and hexadecyl cis-10-tetradecenoate Hexadecyl cis-9-tetradecenoate commonly known as Cetyl myristoleate (CMO) is being used for the treatment of osteoarthritis and other joint inflammatory diseases, cis-9- Tetradecenoic acid (cis-9-myristoleic acid) is the main precursor for the preparation of CMO. As there are limited natural plant sources for cis-9-tetradecenoic acid, the present invention aimed at the synthesis of cis-9-tetradecenoic acid methyl ester from oleic acid methyl ester. As oleic acid is not available in pure form, this has to be isolated from oleic acid-rich oils like olive oil. cis- 10-Tetradecenoic acid methyl ester, an isomer of cis-9-tetradecenoic acid was also prepared from undecenoic acid methyl ester, a derivative of castor oil. Undecenoic acid is easily available commercially in pure form. Hexadecyl cis-9-tetradecenoateand hexadecyl c/s-10-tetradecenoate were prepared by enzymatic transesterification of cis-9-tetradecenoic acid methyl esterand cis-10- tetradecenoic acid methyl ester with 1-hexadecanol (cetyl alcohol) respectively. Both the isomers of cetyl myristoleate were evaluated for anti arthritis, blocking inflammation and reduction of adjuvant-induced arthritis in rats.
WO2012048330A2 Treatment of motor neuron disease Provided herein are methods and compositions for the treatment of motor neuron diseases including, for example, amyotrophic lateral sclerosis. Suitable therapeutic agents include, for example, agents that up-regulate the expression IGF-II or guanine deaminase in a cell.
US20100256191 Ampa receptor antagonists and zonisamide for epilepsy The invention provides methods for treating epilepsy by administering to patients therapeutically effective amounts of AMPA receptor antagonists in combination with zonisamide useful for treating epilepsy. The invention also provides pharmaceutical combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists, and optionally, zonisamide that are useful for treating epilepsy.
US20090143384 2,4,6-Trisubstituted Pyrimidines as Phosphotidylinositol (Pi) 3-Kinase Inhibitors and Their Use in the Treatment of Cancer The invention concerns pyrimidine derivatives of Formula (I) wherein each of Qa, G1, G2, q, R3, r, R4, X1 and Qb have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.
WO2014107566A1 Surface binding of nanoparticle based drug delivery to tissue Microparticles and nanoparticles and compositions thereof are provided. The microparticles and nanoparticles and compositions may be used for the treatment of musculoskeletal disease, such as osteoarthritis and injury such as trauma.
CN102940857A Medicine composition for treating depression and preparation method thereof The invention discloses a medicine composition for treating depression and a preparation method thereof. The medicine composition comprises the following ingredients in parts by weight: 1-2 parts of saikosaponin, 1-2 parts of radix curcumae volatile oil and 1-3 parts of pachymaran. The preparation method of the medicine composition for treating depression comprises four steps of raw material preparation, raw material weighing, raw material inclusion and medicine mixing and forming. The medicine composition is prepared by combining active ingredients of natural medicinal raw materials or extracts of the active ingredients of the medicinal raw materials, and has the advantages that the medicine composition has good curative effects and no toxic or side effects, is not easy to generate tolerance, is universally suitable for depression patients, etc. Being prepared from the extracts of the active ingredients, the medicine composition is taken without decoction, can be applied to the patients by oral administration, suction or parenteral administration, can be prepared into tablets, capsules, powder, granules, syrup or oral liquid and the like, and is convenient to carry and take.
EP1169029B1 Use of sibutramine or its derivative for the treatment of sleep disorders A compound of formula (I) or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl, including individual enantiomers or racemates thereof, (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine hydrochloride optionally in the form of its monohydrate) is used for treating sleeping disorders including sleep apnoea and snoring.
US20110200645 DHA Free Fatty Acid Emulsions The present invention is directed to an emulsion comprising an emulsifier, an isotonic agent and a docosahexaenoic acid free fatty acid (DHA-FFA) wherein the emulsion is substantially free of eicosapentaenoic acid (EPA) and is suitable for parenteral administration.
WO2006113650A1 Design and synthesis of novel tubulin polymerization inhibitors: bonzoylphenyluria (bpu) sulfur analogs A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 µM.
US20080268053 Collagen carrier of therapeutic genetic material, and method A collagen matrix material is charged with a cell growth-promoting derived nucleic acid sequence. The nucleic acid sequence-charged collagen matrix material may be utilized in a method of promoting regeneration of surface cartilage of a joint. In the method, an area of injury is covered with the nucleic acid sequence-charged collagen matrix material, the collagen matrix material is fixed over the area to be treated, and the area is allowed to heal.
US20080311122 Antagonists of Hmgb1 and/or Rage and Methods of Use Thereof Compositions and methods are disclosed for inhibiting the release of a proinflammatory cytokine from a vertebrate cell, and for inhibiting an inflammatory cytokine cascade in a patient. The compositions comprise, for example, high affinity antibodies that specifically bind HMG1 and antigenic fragments thereof. The high affinity antibodies of the present invention and pharmaceutical compositions comprising the same are useful for many purposes, for example, as therapeutics against a wide range of inflammatory diseases and disorders such as sepsis, rheumatoid arthritis, peritonitis, Crohn s disease, reperfusion injury, septicemia, endotoxic shock, cystic fibrosis, endocarditis, lupus, psoriasis, psoriatic arthritis, arthritis, anaphylactic shock, organ ischemia, reperfusion injury, and allograft rejection. In addition, the high affinity antibodies of the present inventions are useful as diagnostic antibodies.
DE102010014427A1 Combination, to treat e.g. tumors e.g. breast cancer, and psoriasis comprises substituted N-(4-hydrosulfonimidoylphenyl)-5-(trifluorometh yl)pyrimidin-2-amine compounds and antihyperproliferative, cytostatic or cytotoxic substances Combination comprises substituted N-(4-hydrosulfonimidoylphenyl)-5-(t rifluoromethyl)pyrimidin-2-amine compounds (I) and their salts, diastereomers and enantiomers and antihyperproliferative, cytostatic or cytotoxic substances. Combination comprises substituted N-(4-hydrosulfonimidoylphenyl)-5-(t rifluoromethyl)pyrimidin-2-amine compounds of formula (I) and their salts, diastereomers and enantiomers and antihyperproliferative, cytostatic or cytotoxic substances. X : -O- or -NH-; R1 : methyl, ethyl, propyl or isopropyl; R2, R3 : H, methyl or ethyl; and R4 : 1-6C-alkyl or 3-7C-cycloalkyl ring. [Image] - ACTIVITY : Cytostatic; Antipsoriatic; Vulnerary. - MECHANISM OF ACTION : Pan-cyclin dependent kinase (CDK) inhibitor.
EP2087887A1 Highly absorbable composition for oral administration containing oxidized coenzyme q10 The present invention provides a method of increasing the absorbability of oxidized coenzyme Q10 by preparing the oxidized coenzyme Q10 as a composition in the presence of a lysolecithin and an oil and fat. The composition of the present invention comprising oxidized coenzyme Q10, a lysolecithin and an oil and fat, wherein the weight ratio of the lysolecithin to the oxidized coenzyme Q10 is not less than 0.7, shows superior absorption of oxidized coenzyme Q10 and can be utilized for food, food with nutrient function, food for specified health uses, nutritional supplement, nutritional product, animal drug, beverage, feed, pet food, cosmetics, pharmaceutical product, therapeutic drug, preventive drug and the like.
US20100311788 Salts of Clopidogrel With Polyanions and Their Use for Manufacturing Pharmaceutical Formulations The invention relates to salts of the active ingredient clopidogrel with polyanions. The salts are predominantly in amorphous form, and the polyanions have at least 4 negative charges.
US6974807 administering topically to alleviate proliferative skin diease; nontoxic The present invention provides a method for treating proliferative skin diseases comprising the administration of an effective amount of tazarotene and an effective amount of a corticosteroid. This invention is especially useful for treating psoriasis.
CN101284129A Composition containing lactase and vitamin D The invention relates to a composition mainly containing lactase and vitamin D. The composition is mainly used for improving lactose intolerance and promoting calcium absorption. The composition is mixed with proper adjuvants, and then preapred into a plurality of oral products such as conventional tablet, effervesce, buccal tablets, milk tablet, orally disintegrating tablet, granule, effervescent granule, powder, capsule and soft capsule.
WO2006085655A1 Ointment An ointment comprising an oleagenous base and a compound of the formula: (I) wherein R1 is any of group of the formula -(CH2)4-S-CH2-CO2H, group of the formula -(CH2)4-S-CH2-CO2CH3, group of the formula -(CH2)4-C≡C-CO2H, group of the formula -CH2-S-(CH2)2-S-CH2-CO2H and group of the formula -CH2-S-(CH2)4-CO2H. This ointment is one containing a compound effective in atopic symptoms, and is low in skin irritation and excels in storage stability to thereby be usable as a pharmaceutical effective in itching attributed to atopy, etc.
CN1927182A Procyanidins nano milk-like liquid medicine and its preparation The invention discloses a procyanidin nanoemulsion drugs the composition of which is procyanidin, non-ionic surfactant, oil, deionized water, its preparation method is surfactant is loaded and weighed according to the proportion formula, choosing oil phase, and make sure that the HLB for its emulsion is close to the HLB of surfactant, then well prepared surfactants and oil phase is mixed according to the original proportion formula, adding proportional anthocyanin, blending and stirring completely, slowly dropwising deionized water and stirring at room temperature until it has similar viscosity with water and become clear transparent solution which is procyanidin nanoemulsion drug. Nano-procyanidin significantly improves the solubility, dispersion of procyanidins in water and its bioavailability, improves the stability of procyanidins. The nano-emulsion can be widely used in cosmetics, pharmaceuticals, beverages, health care products, fodder and other fields.
CN102838464A New compound selaginellin N with anticancer activity, and uses thereof The present invention belongs to the technical field of medicine, and discloses a structure of a new alkyne phenol compound selaginellin N with natural anticancer activity, and uses of the compound selaginellin N in cancer treatment. A chemical name of the compound is (R,S)-4-[[4'-hydroxy-3-[2-(4-hydroxyphenyl)ethynyl][1,1'-biphenyl]-2-yl](4-methoxyphenyl)methylene]-2,5-cyclohexadien-1-one. With in vitro culture method screening experiments, results of in vitro anticancer activity tests show that selaginellin N provides significant inhibition activity for three selected human tumor cell lines. According to the present invention, specific data comprises that: the compound selaginellin N provides a strong killing effect for U251 glioma cells, wherein IC50 is 23.52-27.16 mug/mL; the compound selaginellin N provides a strong killing effect for HeLa cervical cancer cells, wherein IC50 is 21.48-23.54 mug/mL; and the compound selaginellin N provides a strong killing effect for MCF-7 human breast cancer cells, wherein IC50 is 31.52-36.16 mug/mL.
WO2007143582A2 Reversal of the suppressive function of specific t cells via toll-like receptor 8 signaling CD8+ regulatory T (Treg) cells and γδ Treg cells profoundly suppress host immune responses and thus protect against autoimmune disease while restricting desired immune responses such as antitumor immunity. Synthetic phosphorothioate-protected, guanosine- containing oligonucleotides can directly reverse the suppressive activity of Treg cells without involving dendritic cells. This effect appears to be transduced by signaling through Toll-like receptor (TLR) 8 and engagement of the MyD88 and IRAK4 molecules in Treg cells, in specific embodiments. Stimulation of Treg cells with natural ligands for human TLR8 recapitulated the effect of the synthetic guanosine-containing oligonucleotides.
CN1947707A Floated in staomach type slow-release tablets contg. berberine hydrochloide and its prepn. method A floating-in-stomach slow-release tablet of berberine hydrochloride for treating gastritis, gastric ulcer and duodenal ulcer is prepared from berberine hydrochloride, carbomer, hydroxypropyl cellulose, acrylic resin No.2 and No.3, calcium carbonate, povidone K30, carboxymethyl cellulose sodium, and polyethanediol through granulating and tabletting.
US7279498 Substituted aryl amides as IP antagonists Compounds effective as IP receptor modulators, particularly IP receptor antagonists, that are of the formula I: wherein A, R1, R2, R3 and R4 are as defined in the specification; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
CN1732972A Dextran for injection and method for preparing the same The invention provides a dextran for injection and its preparing process, which comprises dextran freeze-dried powder or asepsis powder 1-25g, preferably 6-15g. The freeze-dried injection can also contain excipient, auxiliary solvent, pH modifier, and stabilizing agent including oxidation resistant and metal chelating agent.
WO2013062073A1 Orally disintegrating tablet containing low-dose ramosetron The purpose of the present invention is to provide an orally disintegrating tablet which contains low-dose ramosetron or a pharmaceutically acceptable salt thereof and has biological equivalence to conventional tablets. Provided is an orally disintegrating tablet comprising ramosetron or a pharmaceutically acceptable salt thereof in an equivalent molar amount to 0.001 to 0.05 mg inclusive of ramosetron hydrochloride and an agar and/or an agar powder.
CN101891752A Prodrug of DCK (deoxycytidine kinase) analogue, preparation method and application thereof The invention relates to a prodrug of DCK (deoxycytidine kinase) analogue, a preparation method and application thereof. In particular, the prodrug of the invention is a compound shown as the formula I, or salt, solvate and crystalline thereof acceptable in pharmacy; all variables are described in the specification. The invention further relates to a method for preparing prodrug, a prodrug-containing pharmaceutical composition and application thereof in resisting HIV. The prodrug of the invention is applied to treating diseases or symptoms relative to the HIV infection.
CN101896069A Enhancement of plant growth Treatment with N-(2-phenylethyl)succinamic acid or its salts protects against inhibition of growth by a neonicotinoid compound applied as a seed treatment or applied directly on or near the root zone of the seedling.
EP2283017A1 Fused pyrimidineone compounds as trpv3 modulators The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRP V3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
US20110178075 Indoles, 1h-indazoles, 1,2-benzisoxazoles, 1,2-benzoisothiazoles, and preparation and uses thereof The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
US20080206360 Riboflavin (vitamin B2), extract of feverfew, magnesium, magnesium oxide, vitamin B6, B12, betaine, and plant derived phytochemicals Formulations for the prevention and treatment of headaches, particularly migraine headaches, comprise folate in combination with one or more of riboflavin, feverfew, or an extract of feverfew, magnesium in the form of acid salts, magnesium oxide, complexes or chelates and/or other nutritional supplements such as vitamin B6, B12, betaine, and plant derived phytochemicals or synthesized versions thereof.
US20060052594 New corticosteroids Nitrooxy derivatives of steroidal compounds of general formula B—X1—NO2 (I) or esters or salts thereof, wherein: B is a steroidal radical, X1 is a bivalent linking group comprising an aromatic or heterocyclic ring.
EP0693129B1 Method of inhibiting the transcription of genes The invention concerns the inhibition of the transcription of genes in higher eucaryotic cells by inhibiting the activation of NF- kappa B, the cells being treated with substances which specifically inhibit, directly or indirectly, the proteolytic decomposition of I kappa B- alpha . The invention also concerns a method of screening substances which inhibit NF- kappa B activation by inhibiting the proteolytic decomposition of I kappa B- alpha , as well as the use of such substances to treat pathological conditions attributable to undesirable gene expression controlled by NF- kappa B.
EP1654221A2 Aniline derivatived androgen-, glucocorticoid-, mineralcorticoid- and progesterone- receptor modulators This invention relates to aniline derived non-steroidal compounds that are or are believed to be modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
CN101822636A Slowly released and controlled-drug delivery system of injectable estriol The invention discloses a slowly released and controlled-drug delivery system of injectable estriol, which can conveniently inject the estriol into hypodermis or muscle, has a slowly releasing and controlling effect to the estriol, and plays a part in long efficiency. The system can lead the medicine to be released in human body for a long time after injection, thereby reducing the injection times, having the good patient compliance, and reducing the therapy cost. The slowly released and controlled-drug delivery system of the injectable estriol can select injectable estriol microballoon, injectable estriol micro-capsule, injectable estriol naonparticle, injectable estriol emulsion and injectable estriol in-situ gel.
CN101601654A Hydrochloric acid Fasudil liposome injection and new application thereof The invention discloses hydrochloric acid Fasudil liposome injection and new application thereof. The injection mainly comprises the following components according to parts by weight: 1 part of hydrochloric acid Fasudil, 2 to 20 parts of phospholipid, 0.5 to 10 parts of cholesterol and 1 to 8 parts of polysorbate 80. Simultaneously, the hydrochloric acid Fasudil liposome injection also can be used for treating vertebral artery type cervical spondylosis.
CN101849908A Oral fungi polysaccharide sulfate pro-liposome and preparation method thereof The invention relates to an oral pro-liposome taking sulphating modified fungi polysaccharide as an active ingredient, belonging to the medical field. The fungi polysaccharide, particularly beta-1,3 glucan with a little of 1,6 branching is the main active ingredient of the fungi; after being modified by the sulphating, the fungi polysaccharide has the obvious functions of preventing and curing blood vessel embolism, disseminated intravascular coagulation (DIC), virus infection, hyperlipidemia, and the like. Because the medicine has strong polarity and large molecular weight and is not absorbed by oral administration, the patients are required to be in hospital for inspection after being injected with the medicines and the side effect of mucosal hemorrhage induced by the medicine is difficult to control. The oral pro-liposome is prepared by the medicine, which overcomes the defect of the unstable liposome suspension, realizes the oral absorption for the medicine and reduces the side effect of mucosal hemorrhage by the slow-control and releasing of the liposome to the medicine. The liposome is prepared by adopting the two methods of a reverse evaporation technique and a film-ultrasonic wave dissolving technique, adding a proper carrier, and vacuum drying or freeze drying the pro-liposome. The technique has simple process and easy control and is easy to enlarge the industrialization.
US20060147437 Use of pigmented retinal epithelial cells for creation of an immune privilege site The present invention relates to a novel in vivo method for creation of a localized immunosuppressive environment in tissue. The method involves the transplanting of pigmented retinal epithelial cells into a mammal thereby producing a localized immunosuppressive environment. The transplanted pigmented retinal epithelial cells may also be used to produce therapeutic proteins or other biologically active molecules that may be useful in treatment of diseases.
CN101104625A Liver targetable adefovir precursor medicament and medical use thereof The invention aims at providing a prodrug of adefovir represented by the formula I and non-toxic and pharmaceutically acceptable salt of the adefovir. Wherein, R is alkyl of C1 to C8 or alkyl of C1 to C3 replaced by phenyl.
US20080176796 screening for selective antagonists or agonists of tumor necrosis factor receptors, used as antiinflammatory or antiischemic agents; treatment of cardiovascular and kidney diseases This invention relates to the identification and characterisation of specific cellular responses which are associated with tumour necrosis factor receptor 1 (TNFR1) and tumour necrosis factor receptor 1 (TNFR2). Selective modulation of these tumour necrosis factor receptors (TNFRs) Selective modulations of these responses may be useful in the promotion or inhibition of cell growth, for example, in the treatment of disease conditions, including cardiovascular and kidney diseases. Therapeutic methods employed selective TNFR1 and TNFR2 modulators are provided, along with screening methods for the identification of selective TNFR1 and TNFR2 modulators useful in such methods.
US7078053 Ibuprofen composition Fumaric acid is added in amounts sufficient to reduce the burn sensation commonly associated with propionic acid derivatives.
CN1839881A Trauma-treating mineral The invention provides a mineral substance for treating trauma, which is prepared from unslaked lime and cement through combination, wherein the combination of the substances can produce synergic actions for the effective treatment of trauma.
US7368254 Lipid-based systems for targeting diagnostic agents The invention relates to targeting of diagnostic agents by use of lipid-based compositions. The invention is useful in the diagnosis of various disorders which are associated with or resulting from increased levels of extracellular PLA2 activity in the diseased tissue, e.g. cancer, infectious, and inflammatory conditions.
WO2007083823A1 Androgen receptor-binding activity of genoderma mushroom-treated product Disclosed is an androgen receptor-binding substance comprising an extract from a Ganoderma mushroom (Ganoderma lucidum) as an active ingredient. The androgen receptor-binding substance is useful as a reagent for use in the study on signaling through an androgen receptor or a therapeutic agent for an androgen-dependent disease or an androgen receptor-related disease.
WO2008135639A3 Novel useful inhibitors The invention relates to a method for identifying therapeutic lead compounds useful in treating, preventing and/or alleviating disorders related to PHD3-induced aggresome formation. The invention further relates to pharmaceutical compositionsand methods for detecting PHD3- induced disorders.
EP2404895A1 Calixarene-based peptide conformation mimetics, methods of use, and methods of making A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.
WO2013144129A1 Novel 4-methyl-dihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection The invention provides novel compounds having the general formula (I): wherein R1, R2, R3, R4, R5, M and X are as described herein, compositions including the compounds and methods of using the compounds.
US20110014219 Norovirus and Sapovirus antigens Immunogenic compositions that elicit immune responses against Norovirus and Sapovirus antigens are described. In particular, the invention relates to polynucleotides encoding one or more capsid proteins or other immunogenic viral polypeptides from one or more strains of Norovirus and/or Sapovirus, coexpression of such immunogenic viral polypeptides with adjuvants, and methods of using the polynucleotides in applications including immunization and production of immunogenic viral polypeptides and viral-like particles (VLPs). Methods for producing Norovirus- or Sapovirus-derived multiple epitope fusion antigens or polyproteins and immunogenic compositions comprising one or more immunogenic polypeptides, polynucleotides, VLPs, and/or adjuvants are also described. The immunogenic compositions of the invention may also contain antigens other than Norovirus or Sapovirus antigens, including antigens that can be used in immunization against pathogens that cause diarrheal diseases, such as antigens derived from rotavirus.
EP1951717A1 Novel pyrrolidine derivatives as inhibitors of coagulation factor xa The invention is concerned with novel pyrrolidine derivatives of formula (I) wherein X, Y, R1, R2 and R3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
WO2007094312A1 Agent for promoting vitamin c transporter production It is intended to provide a substance having an action of promoting vitamin C transporter production. An agent for promoting vitamin C transporter production contains, as an active ingredient, a compound of marrubiin, cholesteryl benzoate, ugaferin, rapiferin, geranyl acetate, nerolidol, dihydrojasmone, carbacryl acetate, guaizulene, dihydroconiferyl alcohol, stevioside, DL-alpha pyrene, verbenalin, 1-heptacosanol, 4-hydroxycoumarin, cholic acid, cholesteryl oleate, fraxin or bergaptol, or an extract of Magnolia obovata, almond, Hydrangea macrophylla, grapefruit, Ophiopogon japonicus, Hedera helix L, Saponaria officinalis L., Houttuynia cordata, chamomile, Uncaria gambir, hamamelis, Morus alba, rice bran or field horsetail.
US20130024961 Methods of Modulating Thrombocytopenia and Modified Transgenic Pigs The application provides methods of modulating platelet uptake by liver sinusoidal endothelial cells and of modulating thrombocytopenia. Transgenic pigs modified to bind fewer platelets are provided.
CA2338311C Prodrugs of the pyridyl methyl sulfinyl benzimidazoles Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolysable sulfinyl or arylsulfonyl group attached to the benzimidazole nitrogen, or include a group that forms a Mannich base with the benzimidazole nitrogen. The prodrugs of the invention hydrolyse under physiological conditions to provide the proton pump inhibitors with a half life measurable in hours, and are capable of providing sustained plasma concentrations of the proton pump inhibitor drugs for longer time than presently used drugs.The generation of the proton pump inhibitor drugs from the prodrugs of the invention under physiological conditions allows for more effective treatment of several diseases and conditions caused by gastric acid secretion. A prodrug of the invention has the general formula Het1-X-S(O)-Het2.
WO2010118207A1 Pyrazolo [1, 5-a] pyrimidine derivatives as mtor inhibitors The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.
US7585863 Antitumor agents; such as (2-(4-(7-Chloro-2-quinoxalinyl)oxy)propionylamino ethansulfonic acid; {2-{4-(7-Chloro-quinoxalin-2-yloxy)-phenoxy}propionyl amino}acetic acid The invention provides compounds of the formula: wherein A, X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions comprising a compound of the above formula or a salt thereof, intermediates useful for preparing a compound of the above formula, and therapeutic methods comprising administering a compound of the above formula or a salt thereof to a mammal in need thereof.
US20110015227 Warming sensate composition The invention relates to a warming sensate composition of (i) a hot component, (ii) a cooling component, and (iii) optionally a bitter component. The weight ratio of (i):(ii) is from 1:3 to 1:100. If a solvent is provided in the composition, the solvent is present in an amount of less than 10 wt % ethanol, based on the total weight of the composition. Also, the bitter component, when used, is present in an amount of less than 0.15% by weight based on the total weight of the composition.
EP1084710B1 Adenosine a1 antagonists for male sterility Efficacious remedies for male sterility which are in the form of preparations containing as the active ingredient an adenosine A1 antagonist.
EP2721003A1 Nuclear receptor modulators and their use for the treatment and prevention of cancer Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R1 to R5 and X1 to X5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.
CN103565994A Medicine for treating gouty arthritis and preparation method of medicine The invention discloses a medicine for treating gouty arthritis and a preparation method thereof. The medicine is mainly prepared from cortex phellodendri, strychni semen, rhizoma atractylodis, radix achyranthis bidentatae, caulis piperis kadsurae, caulis sinomenii and prepared common monkshood daughter root according to a certain weight proportion. The medicine has functions of promoting blood circulation to remove blood stasis, expelling wind-damp, dredging meridians, nourishing liver and kidney and strengthening muscles and bones, and has the advantages of quickly taking effect, having a good curative effect and no relapse for treating the gouty arthritis.
EP1720543A1 Roflumilast and glycopryrronium combination This invention relates to pharmaceutical formulations containing combinations of roflumilast and a pharmaceutically acceptable salt of glycopyrronium and the use of such pharmaceutical compositions in medicine, in particular in the prophylaxis and treatment of respiratory disease.
WO2011049954A3 Compositions comprising wnt modulators or neurotoxins for the treatment of otic disorders Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with otic agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).
US7358252 Psychological disorders; central nervous system disorders; antidepressants; anxiolytic agents; stress reliever Corticotropin releasing factor (CRF) antagonists of Formula (I): and its use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
US7312360 Substituted hydroxyethylamines Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables G, L, A, W, E, R2, R3, R4, R5, RN, and Rc are defined herein. These compounds interact with and inhibit the activity of the enzyme beta-secretase. These compounds are therefore useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions and methods of treatment of these diseases are also disclosed.
WO2006109737A1 Pranlukast hydrate-containing preparation having relieved bitterness In providing granules containing pranlukast hydrate and a preparation (tablets quickly disintegrating in the oral cavity) containing these granules, the bitterness can be relieved by reducing the average particle diameter of pranlukast hydrate. Moreover, the effect can be improved by specifying the average particle diameter and the bulk density of the granules containing pranlukast hydrate. Namely, the granules containing pranlukast hydrate and tablets containing the granules show a relieved bitterness and can quickly disintegrate. Therefore, they can be provided as preparations having excellent administration properties. It is also possible to provide a high-content preparation wherein the content of pranlukast hydrate is increased while the content of sugars is decreased.
WO2007138961A1 Prophylactic or therapeutic agent for disorder induced by macrophage migration inhibitory factor [PROBLEMS] The major object is to provide a prophylactic or therapeutic agent which is highly effective on a disorder induced by macrophage migration inhibitory factor (MIF) and has few adverse side-effects. [MEANS FOR SOLVING PROBLEMS] It is found that a thioredoxin family polypeptide (TRX) can bind to MIF directly to inhibit the inflammatory activity of the MIF and prevent the incorporation of the MIF into a cell. Therefore, it is concluded that a TRX is effective on a variety of disorders induced by MIF. Provided is a prophylactic or therapeutic agent for a disorder induced by MIF, which comprises at least one TRX or TRX-inducer as an active ingredient.
US20120289479 Materials and Methods Related to Sodium/Potassium Adenosine Triphosphate and Cholesterol This invention is based in part on the elucidation of new structural conformations and functions of the sodium/potassium adenosine triphosphate synthase (Na/K ATPase), and especially elucidation of new binding sites and interactions. The present invention provides practical applications of several surprising structural and functional relationships between Na/K ATPase and compounds which interact with Na/K ATPase. Disclosure of these structures and relationships provides insight and practical solutions to chemically affecting not only the Na/K ATPase interactions, but also regulators known to be upstream and downstream.
CN102850369A Nitrogen monoxide donor-type oridonin 1,4-hydroxyl-modified derivative, and its preparation method and application The invention relates to pharmaceutical chemistry field, and especially relates to a nitrogen monoxide donor-type oridonin 1,4-hydroxyl-modified derivative. The invention also discloses a preparation method for the nitrogen monoxide donor-type oridonin 1,4-hydroxyl-modified derivative and application of the compound in anti-tumor.
CN102526284A Gel with anti-inflammation, anti-pruritus and sterilization effects and preparation method for gel The invention relates to gel with anti-inflammation, anti-pruritus and sterilization effects, and belongs to the field of medicines. The gel is mainly applied to pediatric pruritic dermatosis, and can be used in different forms such as a therapeutic medicament and/or a sterilizer, a health care product, a sanitary product and the like for adjunctive therapy or for different purposes. The invention provides brand-new gel, wherein the gel is prepared by adding pharmaceutically acceptable minor ingredients into the following raw materials in parts by weight: 10 to 20 parts of lonicera japonica (lonicera confusa), 4 to 12 parts of belvedere fruit, 6 to 14 parts of astragalus mongholicus, 1 to 4 parts of lithospermum purpurocaeruleum, 8 to 16 parts of cortex dictamni, 1 to 4 parts of mint, 0.001 to 2 parts of borneol, 1 to 4 parts of cicada slough, 8 to 16 parts of talc, 1 to 4 parts of licorice and 0.1 to 2 parts of honey. By the gel, the effects of dispelling wind, clearing heat, cooling blood, resolving toxin, removing dampness, relieving itching, removing impurities and protecting skin can be effectively achieved; and the gel is particularly applied to the pediatric pruritic dermatosis such as pediatric papular urticaria, miliaria, dermatitis aestivale, diaper dermatitis and eczema.
US20090318556 Biomarkers for detecting radiation exposure: methods and uses thereof Disclosed herein are biomarkers for determining gamma radiation exposure by an animal or human. The biomarkers include 3-hydroxy-2-methylbenzoic acid 3-O-sulfate, N-hexanoylglycine, β-thymidine, taurine, xanthine, xanthosine, 2′-deoxyuridine, 2′-deoxycytidine, 2′-deoxyxanthosine, or any salt, ion, or combination thereof. Also disclosed are methods for determining gamma radiation exposure by an animal or human, which include the step of measuring the amount of one or more biomarkers specific to gamma radiation in the biological fluid and correlating the amount of said biomarkers to the amount of gamma radiation exposure by the animal or human. Systems for determining gamma radiation exposure by an animal or human and methods of treating an animal or human for gamma radiation exposure are also disclosed.
US20090274674 Heterocyclic Oxime Compounds, Process for Their Preparation and Pharmaceutical Compositions Containing Them Compounds of formula (I): wherein: X represents a hydrogen or halogen atom or an alkyl group, R1, R2, R3 and R4 are as defined in the description, A represents an alkylene chain as defined in the description, B represents an alkyl or alkenyl group substituted by a group D represents a pyridine nucleus.
WO2012037393A1 Piperidinyl-substituted lactams as gpr119 modulators Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
US20120052062 Methods for Treatment of Non-Small Cell Lung Cancer The present invention provides methods of treating non-small cell lung cancer by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound in combination with a therapeutically effective amount of an epidermal growth factor tyrosine kinase inhibitor
CN102757435A Trans-3-indolyl-4-pyrroldiazepinecycloheptane-2,5-pyrrolidine-2,5-diketone compound and preparation method thereof The invention relates to the field of chemical synthesis of medicaments, in particular to a trans-3-indolyl-4-pyrroldiazepinecycloheptane-2,5-pyrrolidine-2,5-diketone compound and a preparation method thereof. Research trails on the tumor suppression effect of tumor-bearing mice find that the compound has an obvious tumor suppression effect and can be applied to preparation of anti-tumor medicaments.
EP1716852A1 A composition comprising campothecin or a campothecin derivative and an alkylating agent for the treatment of cancer The present invention relates to therapeutic associations for the treatment of cancer, comprising an effective amount of a campothecin, or a campothecin derivative, with an effective amount of an alkylating agent, such as melphalan, dacarbazine, or cyclophosphamide, and methods of using such therapeutic associations.
US20100008993 Compositions and Methods for Increasing Bioavailability of Topical Ophthalmic Drugs An ophthalmic composition comprises an ophthalmic drug that has a low solubility in water and a surfactant, wherein the ophthalmic drug is present at a concentration from about 3 to about 7000 times the solubility of the drug in water. A volume of about 1-15 microliter is administered topically to an eye of a subject to treat or control a condition for which the drug is effective.
US20100261751 Method for determining one of the two human immunodeficiency virus (hiv) integrase enzymatic activities The invention concerns a method for determining one of the two Human Immunodeficiency Virus (HIV) integrase enzymatic activities, in particular 3′-end processing, in an in vitro assay.
WO2011081383A2 Composition including naphthoquinone compound for treating and preventing hearing loss The present invention relates to a composition including a naphthoquinone compound for treating and preventing hearing loss.
EP2621491A1 2-pyridone antimicrobial compositions Described are a series of 2-pyridone compounds as a potent and selective new class of type II topoisomerase inhibitors with broad-spectrum antimicrobial activity having the general formula (I); where R1, R2, X, and Y are defined herein Such compounds can be used in methods for treating an infection caused by a gram-positive pathogen, a gram-negative pathogen, or a drug-resistant strains thereof.
CN101856322A Sulfadiazine silver controlled-release gel and preparation method thereof The invention discloses sulfadiazine silver controlled-release gel which is prepared by the following method: (1) evenly mixing sulfadiazine silver and sodium alginate aqueous solution into a suspension in darkness, pouring the suspension onto a glass plate mold to make same naturally and smoothly flow, freezing and unfreezing at the room temperature in darkness; (2) adding calcium chloride to water-soluble chitosan solution, and fully mixing until the calcium chloride is dissolved to obtain the water-soluble chitosan-calcium chloride mixture; and (3) immersing the prepared product in step (1) in the water-soluble chitosan-calcium chloride mixture, holding, removing the glass plate mold and rinsing to obtain the sulfadiazine silver controlled-release gel. The sulfadiazine silver controlled-release gel of the invention has good biocompatibility and achieves the effects of stopping bleeding and helping healing; and the sulfadiazine silver controlled-release gel achieves good effect of moisture preservation and is favorable for healing the wound surface and easily applied and removed, thus relieving the pain of the sick and wounded caused by secondary wound.
CA2816551A1 Method of treating mucosal inflammation A method of treating mucosal inflammation associated with a pathological condition in a mammal is provided. The method comprises the step of inhibiting 5-HT signaling at a target site in order to block 5-HT7 receptor function.
CN101648937B Isoflavones compound and preparation and application thereof The invention discloses a novel isoflavones compound as shown by a formula I. The results of animal experiments show that the isoflavones compound can significantly inhibit the proliferation of T cells and B cells, and can be used for preparing immunosuppressants or medicaments for treating immunologic diseases. The SI values (IC50/CC50) of the isoflavones compound are high, so the toxic side effects of the isoflavones compound are small, and the treatment interval of the isoflavones compound is wide. The isoflavones compound is obtained by extracting and separating clover shrubs, and the preparation method is simple and convenient.
WO2010025251A2 Materials and methods for modulating appetite, weight gain and adhd using varenicline The present invention concerns methods and materials for modulating appetite and weight reduction in persons or animals. The present invention also concerns methods and materials for treating, hyperactivity and attention-deficit disorders, such as ADHD in persons or animals. The subject invention also concerns compositions comprising varenicline, or a pharmaceutically acceptable salt and/or analog thereof, and one or more compounds that suppress or inhibit appetite and/or promote weight reduction in a person or animal. The subject invention also concerns compositions comprising varenicline, or a pharmaceutically acceptable salt and/or analog thereof, and one or more compounds used to treat hyperactivity and/or attention-deficit disorders in a person or animal.
CN1868474A Ebastine tablet and its prepn. method A tablet of Ebastine is prepared from Ebastine, hydroxypropyl cellulose, microcrystalline cellulose, lactose, and adhesive through superfine pulverizing, proportional mixing, granulating, sieving, mixing and tabletting.
CN103230587A Composition of crocodile hemoglobin peptide and preparation method of composition The invention discloses a composition of crocodile hemoglobin peptide and a preparation method of the composition, and aims at providing a composition which has the advantages of reinforcing the human body immunity and the oxidization resistance, reducing the formation number of radicals in a human body and improving the cardiovascular disease. The composition is technically characterized by comprising the following raw materials by weight percent: 1-90 percent of crocodile hemoglobin peptide, 1-50 percent of protein derived from crocodile meat and 1-50 percent of coenzyme Q10, and the percent sum of all components is 100 percent. The preparation method comprises the steps of: 1. weighing the crocodile hemoglobin peptide, the protein derived from crocodile meat, the coenzyme Q10, maltodextrin and an adhesive; and 2. preparing the weighed crocodile hemoglobin peptide and protein polypeptide derived from crocodile meat through a conventional spraying method into fine particles, then mixing with the coenzyme Q10 together, fully mixing, and adding the maltodextrin and the adhesive. The composition belongs to the technical field of biological medicines.
WO2010113957A1 Pharmaceutical composition for treating or preventing glaucoma Provided is a pharmaceutical composition for treating or preventing glaucoma, comprising a pyridylamino acetic acid compound represented by general formula (1) or a pharmacologically acceptable salt thereof as an active ingredient. In formula (1), R1, R2, and R3 each independently represent a hydrogen atom or the like; Y represents a group: -Q1-Q2 (wherein Q1 represents an arylene group or the like; and Q2 represents a group such as an aromatic ring group which may be substituted by a halogen atom or the like) or a dicyclic heteroaromatic ring which may be substituted by a halogen atom or the like; and Z represents a group such as an aromatic ring group which may be substituted by a halogen atom or the like.
WO2007034012A3 Method of obtaining amorphous calcium atorvastatin The invention relates to a novel method of obtaining amorphous calcium atorvastatin from N-phenyl-2-[1-phenyl-2-(4-fluorophenyl)-2-oxo]ethyl-4-methyl-3-oxo-pentanamide (II) and (3R,5R)-7-amino-3,5-(O- isopropylidene)dihydroxy-heptanoate of terc-butyl (III), by reacting same with toluene reflux in the presence of an acid catalyst, using a series of synthesis, isolation and hydrolysis steps, after which the crude amorphous atorvastatin obtained is purified, isolated and dried, said steps being performed under very smooth reaction conditions using very short reaction times, moderate temperatures and minimal amounts of reagents, thereby producing a high-quality product.
CN103127024A Stable disodium adenosine triphosphate tablet The invention relates to a stable disodium adenosine triphosphate tablet, particularly relates to a stable solid pharmaceutical composition containing triphosadenine or medicinal salt thereof, and more particularly relates to the solid pharmaceutical composition, which can highly maintain the content of effective ingredients even if being stored for a long time, is excellent in storage stability, and contains triphosadenine or medicinal salt thereof. The solid pharmaceutical composition disclosed by the invention contains triphosadenine or medicinal salt and calcium salt thereof as the active ingredients, and optional pharmaceutic adjuvant.
WO2009147178A3 Substituted pyridin-2-ylmethylsulphinyl-1h-benzimidaz0les for use in the treatment of brain edema The invention is directed to a new use of substituted pyridyl-2-methylsulfinylbenzinnidazoles for a treatment and/or prophylaxis of brain edema.
US20100184793 Compositions incorporating sesamin-class compounds and vitamin b1 class compounds A composition incorporating at least one sesamin-class compound is enhanced in the anti-fatigue action of sesamin class compounds by additionally incorporating at least one vitamin B1 class compound. Also provided is an anti-fatigue agent containing at least one sesamin-class compound and at least one vitamin B1 class compound as the active ingredients.
WO2013169633A1 Antibacterial calcium-based materials A preparation at least useful as a bone implant is provided, which contains a solid component including a lithium compound and a calcium compound. The preparation shows an anti-bacterial ability in comparison with a preparation contains the calcium compound but free of the lithium compound.
CN1846693A Control released permeation bump tablet of venlafaxine hydrochloride and its prepn process The present invention discloses one kind of osmotic pump controlled release tablet of venlafaxine hydrochloride. The tablet consists of medicine core of venlafaxine hydrochloride and semipermeable film coating with small holes. The medicine core consists of venlafaxine hydrochloride in 75 weight portions, stuffing in 30-250 weight portions, osmotic pressure promoter in 1-50 weight portions, adhesive in 1-20 weight portions and lubricant in 0.1-20 weight portions. The semipermeable film coating consists of semipermeable film coating material in 5-15 weight portions and plasticizer in 1 weight portion. The tablet has excellent release controlling effect, high safety and good patient dependence. The present invention also discloses the preparation process of the osmotic pump controlled release tablet of venlafaxine hydrochloride.
CA2651285C Methods and compositions for treatment of human immunodeficiency virus infection with conjugated antibodies or antibody fragments The present invention concerns methods and compositions for treatment of HIV infection in a subject. The compositions may comprise a targeting molecule against an HIV antigen, such as an anti-HIV antibody or antibody fragment. The anti-HIV antibody or fragment may be conjugated to a variety of cytotoxic agents, such as doxorubicin. In a preferred embodiment, the antibody or fragment is P4/D10. Other embodiments may concern methods of imaging, detection or diagnosis of HIV infection in a subject using an anti-HIV antibody or fragment conjugated to a diagnostic agent. In alternative embodiments, a bispecific antibody with at least one binding site for an HIV antigen and at least one binding site for a carrier molecule may be administered, optionally followed by a clearing agent, followed by administration of a carrier molecule conjugated to a therapeutic agent.
CN103622822A Preparation method and product of azlocillin sodium powder injection The invention discloses a preparation method and a product of azlocillin sodium powder injection. The preparation method comprises the following steps of: screening and disinfecting raw powder of azlocillin sodium to obtain sterile raw powder of azlocillin sodium; transferring the sterile raw powder of azlocillin sodium into a cleaning area to standby; cleaning and sterilizing bottles used for subpackaging the raw powder of azlocillin sodium, and transferring into the clean area to standby; subpackaging the sterile raw powder of azlocillin sodium into the sterile bottles; covering butyl rubber stoppers; pressing aluminum covers to seal to obtain the azlocillin sodium powder injection. According to the method, azlocillin sodium particles are preferred, therefore, the problem of the prior art that azlocillin sodium is difficulty subpackaged is effectively overcome, and the stability of a preparation is improved obviously; the performance detection test shows that the prepared powder injection has high quality, and all detection indexes do not vary obviously after long-term test of more than 12 months and all meet the quality standard, namely, the preparation is high in stability.
WO2013052647A2 Formulations and uses of retinoic acid receptor selective agonists The invention provides retinoic acid receptor (RAR) selective agonists and formulations thereof for the treatment of disease or for inducing a medically beneficial effect.
EP1850827A2 Composition for treating and preventing periodontal disease and method of use The present invention is a mixture for treating and preventing periodontal disease comprising acemannan, an immuno-stimulant with tissue repair activity and a hydrated dialkali monometai polycarboxylate 1 : 1 molar ratio of metal-to-complexing agent, such that lysyl oxidase for collagen formation and subsequent tissue repair is activated.
CN1850047A Slow-release preparation containing beta-lactamase inhibitor and cephalosporin and its use The present invention relates to a slow-released preparation containing beta-lactamase inhibitor and cephalosporin. Said slow-released preparation can be made into antibiotic slow-released injection or slow-released implant preparation. Said injection is formed from slow-released microsphere and solvent, the slow-released microsphere contains slow-released auxiliary material and beta-lactamase inhibitor with antibacterial effective dose and cephalosporin, the solvent is special one containing suspension adjuvant of carboxymethyl cellulose sodium, etc. and its viscosity is 100 cp-3000 cp (20 deg.C-30 deg.C). The slow-released auxiliary material is selected from EVAc, polylactic acid copolymer, sebacic acid copolymer, albumin glue and gelatin, etc. The slow-released implant preparation is prepared by using slow-released microsphere or adopting melting process. Said invention also provides its application method. and can obtain obvious therapeutic effect for curing various infective diseases.
WO2014053965A1 Tropomyosin-related kinase inhibitors The present invention relates to compounds of Formula (IA) and (IB) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
CN101961312A Lipoid acid composition for injection The invention discloses a lipoic acid composition for injection, which is an injection and comprises the components of lipoic acid, a compatibilizer and an antioxidant. The disclosed lipoic acid composition has high stability by taking methionine as the antioxidant.
US6991776 Halogenated xanthene or halogenated xanthene derivative; cancer treatment New intracorporeal radiodense medicaments and certain medical uses and methods for use of such high energy phototherapeutic medicaments for treatment of human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene or halogenated xanthene derivative. The halogenated xanthenes constitute a family of potent radiosensitizers that become photoactivated upon irradiation of the treatment site with ionizing radiation. In embodiments of the present invention, such medicaments are used for treatment of a variety of conditions affecting the skin and related organs, the mouth and digestive tract and related organs, the urinary and reproductive tracts and related organs, the respiratory tract and related organs, the circulatory system and related organs, the head and neck, the endocrine and lymphoreticular systems and related organs, various other tissues, such as connective tissues and various tissue surfaces exposed during surgery, as well as various tissues exhibiting microbial or parasitic infection. In another embodiment, such medicaments are produced in various formulations including liquid, semisolid, solid or aerosol delivery vehicles.
CN1602861A Buccal tablet for treating oral anaerobe infection disease and its manufacturing method The invention discloses a preparation of arteannuin for curing gynecological diseases illness and its producing method, which can effectively solve the problem caused by preparation. The invention discloses made by auxiliary materials, and its producing method is chattering and filtering arteannuin or its derivative separately, which are mixed averagely according to the requirement, then add inhibitory action or killing action made by alcohol and pathogen such as colpitis mycotica and trichomonad, make into particle, dry it, then spray organic acid made by citric acid onto the dried particles, add medical effect into the particle and focus. The invention has scientific and reasonable component, remarkable aromatic, convenient eliminating wetness-evil with drugs of fragrant flavor, advanced producing method.
CN101427993A Prostaglandin microemulsion gel rubber preparation and method of producing the same The invention relates to prostaglandin microemulsion-gel preparation and a preparation method thereof. The preparation comprises prostaglandin E1 or the derivative thereof, oil, emulsifier, assistant for emulsifying agent, gel substrate and water, and also possibly comprises a permeation accelerator, a preparation stabilizer, an antioxidant and antiseptics. The preparation has the advantages of good percutaneous permeability, no stimulation to skin and mucous membrane, simple preparation technique and stable quality, the preparation can be used for treating diseases such as ulcer of limbs caused by erectile dysfunction and chronic arterial occlusion and rest pain of limbs caused by microcirculatory disturbance.
CN102526011A Application of retinoic acid in preparing medicines for curing breast cancer The invention provides application of retinoic acid, namely application of retinoic acid in preparing medicines capable of promoting RXR alpha protein expression of cells and curing breast cancer and application of the retinoic acid serving as biological signs for regulating multiplication of breast cancer. Human breast cancer cells of MDA-MB-231 serve as study objects to observe effects of the retinoic acid on multiplication of breast cancer and effects of ATRA on level of RXR alpha protein expression. Results show that when the concentration of the retinoic acid is more than 100nm/L, and acting time is more than 48 hours, ATRA can restrain multiplication of breast cancer cells and induce expression of RXR alpha to increase.
WO2007148208A2 Carbonylated (aza) cyclohexanes as dopamine d3 receptor ligands The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
CN1723893A 'Huilaxitan' injection, and its prepn. method An injection of aniracetam for intravenous injection is prepared from aniracetam, dissolved by propylene glycol solvent, the mixture of alcohol and water for injection, anti-oxidizing agent and pH regulator.
WO2007071357A2 Pharmaceutical composition comprising (e) -7- [4- (4-fluorophenyl) -6-isopropyl-2- [methyl (methylsulfonyl) amino] pyrimidin-5 -yl- (3r, 5s) -3, 5-dihydr0xyhept-6-en0ic acid A chemically stable formulation of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2- [methyl(methylsulfonyl)amino]pyrim idin-5-yl]-(3R, 5S)-3,5-dihydroxyhept-6-enoic acid or a pharmaceutically-acceptable salt thereof for oral use, such as tablets, capsules, powders, granules has been developed using the substances which stabilize against formation of degradation products: lactone and oxidation product.
CN103623059A Medicine composition and application thereof, and medicament containing medicine composition The invention discloses a medicine composition and application thereof, and a medicament containing the medicine composition. The medicine composition comprises moraceae morus plant total alkaloids and balsam pear total saponins, wherein the mass content ratioof the moraceae morus plant total alkaloids and the balsam pear total saponins is 1:2-7:1; the moraceae morus plant total alkaloids are used in the form of moraceae morus plant extracts in the medicine composition, and the balsam pear total saponins are used in the form of balsam pear extracts in the medicine composition; the moraceae morus plant total alkaloids comprise 1-deoxynojirimycin, and the mass content of the 1-deoxynojirimycin in the moraceae morus plant extracts is 2-50%. Target components are extracted from natural plants; the medicine composition has excellent effects of decreasing blood-glucose, losing weight, and reducing lipid in a synergetic manner, and is particularly suitable for the treating and preventing type 2 diabetes.
US20120328691 Anilinopiperazine derivatives and methods of use thereof The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
CN101703510A Tamsulosin and finasteride compound sustained release tablets and preparation method thereof The invention relates to compound sustained release tablets taking tamsulosin and finasteride as medicinal active ingredients, wherein the tamsulosin can also exist in the form of other pharmaceutically acceptable salts. The preparation also comprises one or more pharmaceutically acceptable sustained release carriers and auxiliary materials consisting of conventional preparations besides main components. The compound sustained release tablets have the advantages of good therapeutic effect, fewer side effects, and safe and reliable use, can maintain steadier blood drug concentration and longer action time due to the sustained release of the medicament, and can be used for the treatment of benign prostatic hyperplasia (BPH).
CN102091189A Gynecological gel The invention discloses gynecological gel, which is mainly prepared from the following raw materials in part by weight: 3 to 20 parts of gallic acid, 5 to 15 parts of himalayan mayapple, 3 to 8 parts of echinacea purpurea extract, 4 to 11 parts of morinda citrifolia extract, 3 to 9 parts of propolis, 1 to 19 parts of Chinese globeflower flower, 8 to 20 parts of rhodiola, 7 to 17 parts of lightyellow sophora root, 3 to 12 parts of realgar, 3 to 8 parts of coptis, 4 to 13 parts of saffron, 2 to 6 parts of vitamin E and 2 to 8 parts of borneol. While curing diseases, the gynecological gel avoids destroying environment of the genital tract, killing beneficial bacteria, arousing medicine resistance and tolerance and wounding human bodies. The gynecological gel disclosed by the invention is more suitable and safer to use, can reduce damage caused by the toxic and side effect of medicines to human bodies, and can improve the immunity of human bodies to protect patients against the toxic and side effect of the medicines.
US20080241147 Using pleckstrin homology (PH) domain-interacting protein as tool in detection and identification of modulators for prevention and treatment of cell proliferative disorders The invention relates to nucleic acid molecules of a Pleckstrin Homology (PH) Domain-Interacting Protein, proteins encoded by such nucleic acid molecules; and uses of the proteins and nucleic acid molecules in the preparation of therapeutic and diagnostic agents. The proteins, nucleic acids molecules, and agents may be used in the diagnosis, prevention, and treatment of conditions and disorders involving the proteins and nucleic acid molecules including but not limited to cancer, and disorders associated with insulin response.
US20070203184 Novel Indolin-2-one Derivatives, Their Preparation and the Pharmaceutical Compositions Comprising Them The present invention relates to novel indolin-2-one derivatives of formula: to the preparation and to the pharmaceutical compositions comprising them. These compounds have an affinity for oxytocin receptors.
CN102525966A Tablet containing paroxetine and preparation method thereof The invention discloses a tablet containing paroxetine and a preparation method thereof. The tablet is composed of paroxetine hydrochloride and auxiliary materials accepted in pharmacy and prepared in a wet granulation process, thereby not affecting tablet manufacturing modes and guaranteeing quality and stability of tablets. The tablet is simple in preparation method, wide in application scope, convenient to transport and store and suitable for scale production. The preparation method is convenient to operate.
CN103041392A Composition of oryzanol and proton pump inhibitor The invention provides a composition of oryzanol and a proton pump inhibitor. The composition includes a clinical effective dose of proton pump inhibitor and an effective dose of oryzanol which are existent in different drug release units respectively; in a unit preparation, the clinical effective dose of proton pump inhibitor is 10-100 mg and the effective dose of oryzanol is 100-500 mg; the proton pump inhibitor in the composition is selected from omeprazole, lansoprazole, pantoprazole, rabeprazole, esomeprazole or pharmacologically suitable racemes, alkaline salt forms or single corresponding isomer forms thereof; and the drug release unit where the proton pump inhibitor is also includes an alkalizer. The composition can be used for treating peptic ulcer.
US7390906 Forming ketone intermediates to terfenadine carboxylic acid metabolite; by use of pure regioisomer of 4-(Cyclopropyl-oxo-methyl)-alpha,alpha-dimethylphenylacetic acid The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.
CN102441170A Methods for administering DPD inhibitors in combination with 5-FU and 5-FU prodrugs The invention provides methods for administering DPD inhibitors in combination with 5-FU and 5-FU prodrugs. Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient.
US20050143456 Carboxamide-substituted phenylurea derivatives, process for their preparation and their use as medicaments The invention relates to carboxamide-substituted phenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and process for their preparation are described. The compounds are suitable, for example, for treating type II diabetes.
US20110105542 Pyrazolo--quinazolines The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C3-C7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C3-C7 cycloalkyl as substituent of a carboxamide at 3 position of the molecula framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
CN101966163A Febuxostat dispersible tablet and preparation method thereof The invention relates to a febuxostat dispersible tablet and a preparation method thereof. The febuxostat dispersible tablet comprises febuxostat as a main material and a diluent, a disintegrant, a binder, a flow aid, a lubricant and other assistants as auxiliary materials, wherein the flow aid is silicone dioxide, and the lubricant is magnesium stearate. The febuxostat dispersible tablet is prepared from the following components in percentage by weight: 5-30% of the febuxostat, 20-80% of the diluent, 5-30% of the disintegrant, 0.1-5% of the binder, 1-10% of the silicone dioxide, 0.2-5% of the magnesium stearate and 2-8% of other assistants. The febuxostat dispersible tablet prepared by adding a proper amount of auxiliary materials into crushed febuxostat has the advantages of rapid and complete drug dissolution and stable quality, is suitable for long-term storage and convenient to use, and the bioavailability of human bodies on drugs is increased so as to increase curative effect.
CA2315115C Compositions of microspheres for wound healing Therapeutic compositions of microspheres for application to wounds and/or lesions for accelerating wound healing and muscle regeneration. The microspheres are made up of non-biodegradable material having a substantial surface charge. The therapeutic composition further includes a pharmaceutically acceptable carrier in which the microspheres are insoluble and a container for holding the composition.The therapeutic composition further contains pharmacologic agents or biologics that accelerate the wound healing process.
WO2007135505A2 Veterinary pharmaceutical compositions for the treatment of pain and inflammation This invention relates to veterinary pharmaceutical compositions based on a combination of tramadol and meloxicam or carprofen for the treatment of pain and inflammation in animals.
CN101874774A Suspension composition containing lysozyme and florfenicol and preparation method thereof The invention relates to a suspension composition containing lysozyme and florfenicol, which is a microemulsion solution prepared from the lysozyme, the florfenicol, tween-80, sodium citrate, methylparaben, propylene glycol and water for injection. The composition adopts compatibility of the lysozyme and the florfenicol, not only enlarges the antimicrobial spectrum, but also has high efficiency, low toxicity, less residues and drug resistance prevention; and the prepared suspension not only can solve the problem that the florfenicol is hardly soluble in water, improves the biological utilization of the florfenicol, but also protects the activity of the lysozyme in gastrointestinal fluid, and plays a slow release effect on the lysozyme and the florfenicol to ensure that the medicament maintains long-term effective blood concentration in vivo, is integrated with instant effect, high efficiency and long action, and can be used for treating mycoplasma gallisepticum infections of livestock and poultry.
CN1895241B Composition of long-acting oral pills of Yansuan Tanshuluoxin and its production method An orally taken long-acting small pill of tamsulosin hydrochloride is proportionally composed of a core, a tamsulosin hydrochloride layer, a first release regulating layer chosen from Youteqi L30D55,Sulisi and kollicoat SR3D, a release assistant layer chosen from alginic acid, microcrystalline fiber and carboxymethyl cellulose sodium, and a second release regulating layer chosen from ethylcellulose, Youteqi L100 and Youteqi S100. Its preparing process is also disclosed.
US20050032837 For therapy of irritable bowel syndrome, drug addiction or dependency, including alcohol addiction, depression, anxiety, schizophrenia, anxiety, schizophrenia and eating disorders The subject invention relates to 4-phenyl-piperidine derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by an opioid receptor. The subject also particularly relates to using such derivatives to treat certain disease states, disorders and conditions, for example irritable bowel syndrome, drug addiction or dependency, including alcohol addiction, depression, anxiety, schizophrenia, anxiety, schizophrenia and eating disorders, among numerous other disease states, disorders and conditions as more fully described herein.
CN102803511A Materials and methods useful for affecting tumor cell growth, migration and invasion It is disclosed herein that miR-221 and miR-222 down-regulate PTEN and TIMP3 tumor suppressors, resulting in TRAIL resistance. The present invention provides research, diagnostic, and therapeutic tools and methods related to this discovery. Diagnostics, prognostics and treatments for human hepatocellular cancer and non-small cell lung carcinoma having a TRAIL resistance are particularly described herein.
CA2255637C Conjugates of cis-docosahexaenoic acid and paclitaxel A composition of matter consisting essentially of a covalent conjugate of cis-docosahexaenoic acid, and paclitaxel; or a covalent conjugate of cis-docosahexaenoic acid and paclitaxel which is associated with a sterile pharmaceutically acceptable carrier and/or an anti cancer agent other than the conjugate.
CN103054813A Azithromycin oral sustained-release dry suspension and preparation method thereof The invention provides an azithromycin oral sustained-release dry suspension and a preparation method thereof. The preparation can overcome the shortcoming of strong bitter taste of an azithromycin oral preparation, continuously and slowly release a medicament for 5-7 days and realize a treatment effect within 7 days after the preparation is taken once. A sustained-release micropill of azithromycin is of the micropill containing the azithromycin, a layer for alleviating taste and a sustained-release layer are further wrapped for preparation, the layer for alleviating the bitter taste is selected from pharmaceutical polymer materials, namely hydroxypropyl methylcellulose, hydroxypropyl cellulose, acrylic acid polymer, polyvidone, polyethylene glycol 4000, citric acid ethyl ester and the like; and the sustained-release layer is selected from the pharmaceutical polymer materials, namely glyceryl behenate, the citric acid ethyl ester, ethyl cellulose, the acrylic acid polymer, the polyvidone, the polyethylene glycol 4000 and the like. The preparation method disclosed by the invention has the advantages of adoption of conventional equipment, original creation of formula process, sweet taste and long sustained-release time. Compared with the ordinary preparation, the medicament has the advantages of long acting time, sweet taste and lasting efficacy, and is particularly suitable for children and easy to accept by patients.
WO2005123132A3 Use of liver-selective glucokinase activators The present invention provides a method of normalizing blood glucose levels in mammals utilizing liver-selective glucokinase activators. The present invention also provides a method of increasing liver metabolism and decreasing apoptosis independent of glucose normalization or hyperglycemic conditions.
CN102500033A Anti-infection venous catheter and preparation method thereof The invention relates to an anti-infection venous catheter and a preparation method thereof. The venous catheter comprises a conduit main body tube, a tip end and a tube seat, and preferably also comprises a connecting seat and a plurality of epitaxial tubes, wherein the parts retained in a human body are the conduit main body tube and the tip end; and an anti-infection medicament rifampicin, an anti-infection medicament minocycline or combination of the two are uniformly loaded on the conduit main body tube. The preparation method of the venous catheter comprises the following steps of: dissolving the anti-infection medicament or the medicament combination to form soak solution; soaking the conduit into the soak solution to fully soak medicaments into the conduit; and drying to remove solvent to prepare the anti-infection venous catheter. During use, the medicaments are slowly released to fulfill the anti-infection aim of the conduit and avoid infection of the conduit during retention in the human body in surgery.
WO2005021518A1 Condensed ring compound and use thereof Compound of the general formula: (I) (wherein all the symbols have the same meaning as in the description). This compound exhibits antagonism against cysLT2 receptor, so that it is useful as, for example, a preventive and/or therapeutic agent for respiratory diseases (for example, bronchial asthma, chronic obstructive lung disease, pulmonary emphysema, chronic bronchitis, pneumonia (e.g., interstitial myositis, etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g., acute sinusitis, chronic sinusitis, etc.), etc.), or as an expectorant agent or cough suppressant.
US20090259167 Methods and compositions for dose-dependent photodynamic therapy of disorders The invention provides methods and compositions for treating a tissue disorder in a subject by parenterally administering a solution of aminolevulinic acid (ALA) or a derivative thereof that is not greater than 1.0 percent by weight into a local subcutaneous or dermal region of the subject; and administering high fluence light to said bodily area to produce a phototoxic species in said local region, thereby treating a tissue disorder in the subject.
US7282498 Substituted fused pyrroleoximes and fused pyrazoleoximes Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.
CA2410253C Regulating lipid levels via the zmax1 or hbm gene The present invention relates to the high bone mass (HBM) gene, the corresponding wild-type gene (Zmax1), and mutants thereof. The genes identified in the present invention are implicated in regulation of physiological lipid levels, and thereby lipid-mediated diseases and conditions. The invention also provides nucleic acids, including coding sequences, oligonucleotide primers and probes, proteins, cloning vectors, expression vectors, transformed hosts, methods of developing pharmaceutical compositions, methods of identifying molecules involved in lipid level regulation in a subject. In preferred embodiments, the present invention is directed to methods for treating and preventing atherosclerosis, arteriosclerosis cardiovascular disease, atherosclerotic and arteriosclerotic associated conditions.
WO2013167985A1 Compositions and methods for the treatment of neurological disorders The invention relates to the compounds of formula (I) and formula (1A) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I) and formula (IA); and methods for treating or preventing neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment, of epilepsy, bipolar disorder, trigeminal neuralgia, attention-deficit, hyperactivity disorder (ADHD), schizophrenia, neuropathic pain, seizures, bipolar disorder, mania, phantom limb syndrome, complex regional pain syndrome, paroxysmal extreme pain disorder, neuromyotonia, intermittent explosive disorder, borderline personality disorder. Myotonia congenita and post-traumatic stress disorder.
CN101439043A Teniposide injection and preparation method thereof The invention relates to the field of medical technology, in particular to a new injection for teniposide mainline and a preparation method of the new injection. Components of the injection include teniposide, Tween 80, phospholipid, a stabilizer and an injection solvent. As no Cremophor EL is contained, compared with existing clinical preparations, not only the teniposide injection has few side effects and good stability and improves the medicine-taking compliance of patients, but also the preparation method of the teniposide injection is simple and easy to operate and the teniposide injection is suitable for large-scale preparation and industrial production.
US7109338 For use in the prophylaxis and the treatment of Picornavirus and human rotavirus infections. The present invention relates to substituted 1,4-dihydro-4-oxoquinolines having antiviral activity. The substituents are present at positions 1, 2 and at least one of 5-8 positions of the quinoline ring.
US20090069439 Use of pargyline for the treatment of hair folliclies Use of Pargyline for the production of a medicament for influencing the metabolism of hair follicles and the modulation of their vital cycle.
US20090181910 Method of prevention and alleviation of toxicity by modulation of irf3 The invention provides compounds, compositions, animal models, drug screening methods, pharmaceutical compositions, and methods of treatment which relate to the modulation of the metabolism of xenobiotic compounds by administering agents which act on IRF3 or an IRF3 control pathway to modulate the activity, expression, or levels of cytochrome P450 enzymes involved in the metabolism of xenobiotic compounds in a subject.
CN101129798B Medical ointment for treating chronic atrophic gastritis by plastering and applying on acupuncture point The invention relates to a medical ointment for treating chronic atrophic gastritis with acupoint application, which solves the treating problem of chronic atrophic gastritis. The medical ointment ismade by astragalus root, campanumaea pilosula, Dendrobium nobile, radix salvia miltiorrhiza, Cinnamomum cassia, beach silvertop root, black plum, citrus fruit, baras camphor, anhydrous adeps lanae, nitrogen ketone and white petrolatum. The preparing method comprises the following steps: disintegrating Cinnamomum cassia; getting aqua aromatic and volatile oil by distilling; getting the extract by reflux-extracting with alcohol and evaporating radix salvia miltiorrhiza; getting the liquid machine by heating, refluxing and extracting astragalus root with alcohol; boiling, depositing with alcoholand evaporating campanumaea pilosula, Dendrobium nobile, radix salvia miltiorrhiza, Cinnamomum cassia and beach silvertop root; getting the extract and merging the above four drugs; adding and mixinganhydrous adeps lanae, baras camphor and white petrolatum; adding nitrogen ketone; getting the medical ointment for treating chronic atrophic gastritis with acupoint application. The invention has the good treatment effect, the high efficient, the low fee, the convenient and safe treatment, which provides creative contribution for treating chronic atrophic gastritis, and makes good fortune for human.
WO2013028543A1 Bax agonist, compositions, and methods related thereto The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.
CN103142646A Application of valproic acid in preparation of multidrug resistance reversal agent of lung cancer resistance medicine The invention discloses application of valproic acid in preparation of a multidrug resistance reversal agent of a lung cancer resistance medicine, and further discloses application of the valproic acid in the preparation of chemotherapeutics sensitizer of lung cancer resistance and a multidrug resistance tumor invasion resisting and transferring medicine. The application of the valproic acid in the preparation of the multidrug resistance reserval agent of the lung cancer resistance medicine verifies that valproic acid has significant function of a cisplatin persister of human lung cancer resistance through experiments, and verifies that the valproic acid can significantly change drug tolerance of a human lung cancer cell to the cisplatin, improve sensitivity of the human lung cancer cell to the cisplatin, and have obvious restraining effect of invasion effect of the persister of the lung cancer cisplatin.
CN102631686A Porous calcium phosphate nano-particle-antisense oligodeoxyncleotide composite as well as preparation method and application thereof The invention discloses a porous calcium phosphate nano-particle-antisense oligodeoxyncleotide composite and relates to the field of medicines. In the porous calcium phosphate nano-particle-antisense oligodeoxyncleotide composite, porous calcium phosphate nano-particles are utilized as the carrier to load survivin antisense oligodeoxyncleotide or survivin antisense oligodeoxyncleotide with fluorescence labeling; and the particle diameter is 30-60nm. The composite manufactured by use of an inverse phase micro emulsion method can be used for mediating the antisense oligodeoxyncleotide into cells and has higher cell transfection efficiency, particularly in vitro Hela cervical cancer cells. The antisense nucleic acid is improved greatly; the tumor cell apoptosis efficiency is promoted; the anti-neoplastic activity is enhanced; the composite can be used for preparing anti-neoplastic medicines, particularly medicines for treating cervical cancer; and the preparation method is simple and rapid.
CA2379282C Amido spiropiperidines promote the release of growth hormone The present invention is directed to certain spiropiperidines of general structural formula (I) wherein R1, R2, R3, R3a, R3b, R4 and R5 are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
US7160888 7-[4-(4-naphthalen-1-yl-piperazin-1-yl)-butoxy]-3,4-dihydro-1H-[1,8]naphthyridin-2-one; use in the treatment of central nervous system disorders, bipolar disorder in a human This invention relates to compounds of the formula 1 wherein G, D, A, Z, Q, X, Y, R1, and R4 through R7 are defined as in the specification, processes for preparing the same and intermediates used in making the same, and pharmaceutical compositions containing such compounds and their use in the treatment of central nervous system disorders and other disorders.
CN103550160A Anti-inflammatory drug powder The invention discloses an anti-inflammatory drug powder. The anti-inflammatory drug powder treats skin diseases caused by bacterial infection in an application mode and is powder formed after grinding of a sulphadiazine tablet. The anti-inflammatory drug powder has the advantages of a good treatment effect and small side effects.
US8410098 N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-OXO-1,2,4-triazin-6-yl]ethyl}butyramide, the preparation method and use thereof Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III and utilized for preparing vardenafil), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound. In the method for preparing vardenafil, a chloro-sulfonation reaction carries out in the early stage of the preparation procedure
US20090143473 Use of inhibitors of the cellular na+/h+ exchanger (nhe) for preparing a medicament for normalizing serum lipids Use of inhibitors of the cellular Na+/H+ exchanger (NHE) for the production of a medicament for the normalization of serum lipids. The active compounds identified as inhibitors of the cellular Na+/H+ exchanger (NHE) are used for the production of a medicament for the normalization of serum lipids. They are used for the production of a medicament for lowering the blood lipid level and illnesses caused thereby, as well as the endothelial dysfunction syndrome and illness caused thereby.
WO2005094842A1 Vitamin b12-containing compositions and methods of use The present invention features compositions that include one or more vitamin B12 compounds and one or more excipients that enhance solubility of the vitamin B12 compounds. In aspects of the invention, the excipients are alcohols, in particular ethanol, propylene glycol, a polyethylene glycol (PEG), glycerol, mannitol, sorbitol, Tween 20, or dimethylsulfoxide or a combination thereof, and/or a salt former. The compositions optionally comprise one or more therapeutic agents other than a vitamin B12 compound. The invention also contemplates processes by which the compositions can be made; kits containing them (or one or more of the components thereof); and methods of using them to treat patients who have a vitamin B12 deficiency, a proliferative disease, an inflammatory disease, or a viral disease.
US20120258981 Process for the Synthesis of Quaternary Amine Compounds The invention relates to a process for the synthesis of quaternized compounds of formula:
CN103349703A Natural pharmaceutical composition, as well as preparation method and use thereof The invention relates to a natural pharmaceutical composition , and a preparation method thereof. The natural pharmaceutical extractive comprises concentrated extractive of water decocted plantain seed- shizandra berry, plantain seed polyose, and shizandra berry polyose according to the proportion of (3-8) : (5-7) : (3-5). The natural pharmaceutical composition has an excellent curative effect on diarrhea related to cancer chemo-treatment and a synergistic effect on cancer chemo-treatment.
US20080221176 treatment of diabetes mellitus, cardiovascular disease, dyslipidemia, artherosclerosis, peripheral vascular disease, inflammation, cancer, and diseases of the central nervous system; 1,1,1,3,3,3-hexafluoro-2-{4-[methyl(phenylmethyl)amino]phenyl}-2-propanol This invention relates to compounds that are modulators of the liver X receptors (LXRs), and also to the methods for the making and use of such compounds.
US20090042867 Compounds for the treatment of alzheimer's disease The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1 to R13, A, B, L, and i are defined as indicated in the description and the claims, as well as the use thereof for treating Alzheimer's disease (AD) and similar diseases.
WO2011047421A1 Antifungal composition and method of treatment of dermatitis An antifungal composition for topical treatment of dermatitis associated with fungal infections comprising a polymer of 2-propenal and a dermatologically acceptable carrier.
EP1762558A1 Process for preparing transcription factors and their use The present invention has an object to develop novel compounds which are effective for the therapy of syndrome X, cancer, myxedema, vascular chronic inflammation and the like, and furthermore prevent/treat the restenosis caused in an artery expansion by a balloon or a stent and have the activity facilitating regenerative medicine by inhibiting rejection of own cells or tissues to be transplanted and the method for preparing the same. Novel acetal derivatives obtained by acylating the hydroxyl group at the 2-position of the orcylaldehyde which ascochlorin and its analogs have and thereafter bonding an alcohol to the aldehyde group in the presence of a basic catalyst are found to achieve the object.
CN201775804U Composite structure of drug for treating type 2 diabetes The utility model relates to a composite structure of a drug for treating type 2 diabetes. The composite structure is characterized by comprising a glipizide osmotic pump tablet core, an outer thiazolidinediones drug layer and a dampproof layer, wherein the dampproof layer is coated outside the thiazolidinediones drug layer; the glipizide osmotic pump tablet core can be a single-layer tablet and also be a double-layer tablet in a push-pull structure; a thiazolidinediones drug is selected from one of pioglitazone or rosiglitazone and pharmaceutically acceptable salts thereof, wherein the glipizide is 2-10 mg, and the pioglitazone is 10-50 mg or the rosiglitazone is 1-10 mg. The utility model combines the advantages of glipizide osmotic pump tablets and glitazones drugs and achieves the purpose of drug combination in a composite structure way.
US20050059725 Treating schizophrenia or Parkinson's disease with thiolutin dioxide The present invention relates to the use of thiolutin dioxide and its derivatives in the manufacture of a medicament. Such medicaments are useful, for example, in the treatment of CNS disorders. The present invention also relates to a process for the production of thiolutin dioxide and its derivatives by fermentation of microorganisms, such as the microorganism Nocardiopsis species ST 100692 (DSM 13834).
US20090186856 Micronutrient phosphates as dietary and health supplements There is provided a dietary or health supplement comprising an effective amount of a micronutrient selected from the group consisting of phosphate derivatives of tocopherol, ubiquinol, ascorbic acid, tocotrienol, retinol and mixtures thereof delivered with an acceptable carrier.
US7351407 Administering agents such as GW-8510, purvalanol A, roscovitine to inhibit expression, signaling or biological functions of connective tissue growth factor The present invention provides a method for lowering intraocular pressure and providing neuroprotection to a patient in need thereof by administering a therapeutically effective amount of at least one non-nucleotide or non-protein agent that inhibits expression and/or signaling of connective tissue growth factor (CTGF).
US20110071195 Novel alkene oxindole derivatives The present invention provides compounds of formula (I), as well as pharmaceutical acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.
WO2012115446A2 Compound based on 5-(substituted alkyl-aminomethyl) isoxazole acting as a t-type calcium channel antagonist The present invention relates to: a compound based on 5-(substituted alkyl-aminomethyl) isoxazole which exhibits pharmaceutical activity with respect to T-type calcium channels; a pharmaceutically acceptable salt thereof; a production method for such a compound; and to a pharmaceutical composition containing such a compound as an active ingredient.
CN1965971A Externally applied compound medicinal tincture for treating intractable tinea and dermatitis and method for preparing same The invention relates to an externally-used medicinal preparation for treating tinea and dermitis and process for its preparation, wherein the raw materials include hibiscus bark, Sichuan aconite root, Kusnezoff monkshood root, jack-in-the-pulpit tuber, pinellia tuber, toad skin, snake slough, asaryl, sulfur, orpiment, white alum, zanthoxylum piperitum, flavescent sophora root, corktree bark, Chinese mugwort leafmulberry leaf, toasted garlic, cow-bezoar, musk ketone, oxytetracycline powder, diphenhydramine powder, chlorpheniramine and vinegar.
EP0925291B1 Spirocyclic dopamine receptor subtype ligands This invention relates to novel, pharmaceutically active compounds of formula (I) wherein a, b and R1 through R6 are defined as in the specification. These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.
CN103212083A Method for preparing stable albumin nano-particles The invention discloses a method for preparing stable albumin nano-particles, belonging to the technical field of biological medicine material preparation. The method comprises the following steps of: carrying out pretreatment on albumin by utilizing non-biotoxic glutathione or cysteine to open intramolecular dithio bonds, precipitating the albumin by using anti-solvents such as alcohol and the like, and carrying out sulfydryl-dithio bond exchange reaction so as to obtain albumin nano-particles with intermolecular dithio bonds. The prepared nano-particles can be used for delivering in-vivo pharmacologically active substances and/or diagnosis aids. The obtained albumin nano-particles have the advantages that the albumin nano-particles not only have good stability under dilution condition, but also have oxidation reduction response in a reduction type environment; and due to such characteristics, the particles can stably exist in in-vivo blood circulation systems of organisms and are degraded under the action of reduced glutathione so as to release the wrapped medicine.
CN101869566A Composition containing small dose of biguanide antidiabetic medicament and statin lipid-lowering medicament and applications thereof The invention relates to a medicament composition containing a small dose of biguanide antidiabetic medicament, statin lipid-lowering medicament and a pharmaceutically acceptable carrier. The invention also relates to the applications of the medicament composition in the preparation of medicaments for preventing or treating diabetes mellitus with hyperlipidemia. The implementation of the invention provides the medicament composition with specific applications, and the medicament composition not only has a precise curative effect, but also can improve the compliance of patients. The patients can take the medicament conveniently, and the medical expense is reduced. The invention has a better market prospect, and belongs to the field of pharmacy.
CN101507732A Preparation capable of preventing and treating oviduct accretion The invention discloses a preparation for preventing and treating fallopian tube adhesion, which consists of the following raw materials according to the weight ratio: 80 to 95g of chitosan with the viscosity of between 1,750 and 2,000Pa.S, and 5 to 20g of metronidazole. The preparation can avoid the adhesion caused by the narrowness of fallopian tube lumens, and can completely avoid the phenomena that the osmotic pressure is affected due to the cellular exudation of fallopian tube walls. The preparation has no side effect, and no complicating disease is found during the use of patients. The preparation provides the treatment with extremely high safety and effective repatency rate for fallopian tube obstruction diseases, solves the problem of fallopian tube adhesion which fails to be solved for a long time in the world, and brings hope for infertile patients caused by fallopian tube obstruction.
WO2009109501A2 Ocular pharmaceutical compositions The present invention relates to novel derivatives of opthalmic compounds for the treatment of ocular diseases.
EP2692719A1 Method for preparing creatine fatty esters, creatine fatty esters thus prepared and uses thereof The present invention concerns a method for preparing a creatine fatty ester or derivative thereof comprising at least one step consisting in reacting a diprotected creatinine with a molecule bearing at least one alcohol functional group and of formula R'-OH in which R' represents a hydrocarbon radical containing at least 4 carbon atoms. The present invention also concerns particular creatine fatty esters or derivative thereof and medical uses thereof.
WO2007042811A1 Pharmaceutical compositions for the treatment of chronic obstructive pulmonary disease The invention relates to the use of a combination of cannabinoids for the treatment of Chronic Obstructive Pulmonary Disease (COPD). Preferably the combination of cannabinoids are cannabidiol (CBD) and delta-9-tetrahydrocannabinol (THC). More preferably the cannabinoids are in a predefined ratio by weight of approximately 1:1 of CBD to THC.
US20100144759 Novel n-(fluoro-pyrazinyl)-phenylsulfonamides as modulators of chemokine receptor ccr4 The invention provides N-(fluoro-pyrazinyl)-phenylsulfonamides of formula (I) wherein R1-R5 are as defined in the specification; processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy
CN103284955A Long-acting progestational hormone controlled-release injection implant and preparation method thereof The invention provides a long-acting progestational hormone controlled-release injection implant. The long-acting progestational hormone controlled-release injection implant comprises the following components according to the total amount of the implant as follows: a) 2-40wt% of progestational hormone and b) 60-98wt% of a mixture of L-polylactide and polylactic acid modified by caprolactone, wherein the weight ratio of the L-polylactide to the polylactic acid modified by the caprolacton ranges from (1: 99) to (99: 1). The invention further provides a preparation method of the injection implant. The injection implant disclosed by the invention can be used for solving a lot of troubles of vast women by orally taking contraceptives, and prolonging the effective time of medicines, so that the pesticide effect and the financial condition are greatly improved, and the result of three months or more than three months of stable controlled release can be realized.
US20100069362 Thienopyrimidone compound The present invention relates to a compound represented by the formula: wherein Ar is an optionally substituted ring; A is a spacer having a main chain of 1 to 4 atoms; B is a bond, a C1-10 alkylene group or an oxygen atom; R3 and R5 are each independently a hydrogen atom or a substituent; R4 is an optionally substituted cyclic group or an optionally substituted C1-10 alkyl group; and R1 and R2 are each independently a hydrogen atom or a substituent, or R1 and R2 or R1 and B are bonded to form an optionally substituted nitrogen-containing heterocycle, or R1 and Ar are bonded to form an optionally substituted nitrogen-containing fused heterocycle, or a salt thereof. The thienopyrimidone compound of the present invention has a superior melanin-concentrating hormone receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of obesity and the like.
CN103585334A Compound diaper ointment A compound diaper ointment comprises raw materials in parts by weight as follows: 5-20 parts of tannic acid, 0.1-0.3 part of sodium sulfite, 5-20 parts of glycerinum, 0.5-1.5 parts of sorbitan monostearate, 1-1.5 parts of radix angelicae, 1-1.5 parts of rheum officinale, 1-1.5 parts of phellodendron amurense and 54.3-85.8 parts of yellow vaseline. A preparation method of the compound diaper ointment comprises the steps as follows: the radix angelicae, the rheum officinale and the phellodendron amurense are ground into fine powder respectively, filtered by a 100-mesh sieve, and then mixed uniformly, so that mixed powder is formed; the glycerinum is taken and heated in water bath, then the sodium sulfite and the tannic acid are added into the glycerinum and dissolved, then the sorbitan monostearate is added into the mixture, stirring is performed, and a mixed raw material is formed; and the yellow vaseline is dissolved and cooled to 60 DEG C, and then the mixed raw material, the mixed powder and the yellow vaseline are uniformly mixed and condensed, so that the compound diaper ointment is obtained. The compound diaper ointment has good effects for treating red hips, diaper rashes and eczema of infants. Raw materials of the compound diaper ointment are prepared reasonably, and the compound diaper ointment has immediate effects and few adverse reactions, is ideal in effect, can protect the safety of the infants to the maximum extent, and is a specialized good product for infant hip protection actually.
US20050209306 Crystalline [R-(R*,R*)]-2-(4-fluorophenyI)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]-1H-pyrrole-heptanoic acid calcium salt (2:1) Novel crystalline forms of atorvastatin calcium designated Fa and Je which are prepared by crystallization from non-aqueous, non-polar solvents at a temperature above 90° C. The crystalline forms are useful as agents for treating hyperlipidemia and hypercholesterolemia.
EP1778622A1 Para-alkyl-substituted n-(4-hydroxy-3-methoxy-benzyl) cinnamamides and the use thereof for producing drugs The invention relates to para-alkyl-substituted N-(4-hydroxy-3-methoxy- benzyl) cinnamamides, to methods for producing them, drugs containing said compounds and to the use thereof for producing drugs.
CN102525952A Method for producing berberine micro-pills The invention relates to a technology for preparing the berberine micro-pills, in particular to a method for preparing the berberine micro-pills. The method comprises the following steps of: adding 1.5 to 2.5 weight parts of wetting agent into 1 weight part of berberine and 0.01 to 25 weight parts of auxiliary materials to prepare a soft material, preparing pill cores by an extrusion rounding technology, drying, and coating on the pill cores, so that the weight of the pill cores is increased by 5 to 20 percent. The berberine micro-pills produced by the production method are easy to take, do not have bitter taste, can be used as intermediate products for producing capsules, granules and suspended agents and also can be subpackaged into finished products directly.
EP0929554B1 Spiro-azacyclic derivatives, their preparation and their use as tachykinin antagonists Substituted spiro-azacyclic derivatives of structural formula (I), wherein R1 represents hydrogen, hydroxy, C¿1-6?alkyl, C2-6alkenyl, C3-7cycloalkyl optionally substituted alkyl, optionally substituted alkoxy, C2-6alkenyloxy, C3-7cycloalkoxy, phenoxy, benzyloxy, cyano, halogen, NR?11COR14, NRaRb, SRa, SORa, SO¿2Ra or OSO¿2R?a; R2 represents hydrogen, halogen, C¿1-6?alkyl or C1-6alkoxy; or when R?2¿ is adjacent to R1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; R4 represents hydrogen, halogen, C¿1-6?alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SR?a, SORa, SO¿2Ra, CO2R?a, CONRaRb, C¿2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy; R5 represents hydrogen, halogen, C¿1-6?alkyl, trifluoromethyl or C1-6alkoxy substituted by C1-4alkoxy; R?6¿ represents hydrogen, CORa, CO2Ra, COCONRaRb, COCO¿2R?a, optionally substituted C¿1-6?alkyl; or R?6¿ represents a group of the formula -CH¿2?C CCH2NR?7R8; or R6¿ represents C¿1-6?alkyl, optionally substituted by oxo, substituted by a 5-membered or 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen atoms optionally substituted by =O or =S and optionally substituted by a group of the formula ZNR?7R8; R9 and R10¿ each independently represents hydrogen, halogen, C¿1-6?alkyl, CH2OR?d¿, oxo, CO¿2R?a or CONRaRb; p is zero or 1; q is 1 or 2; and X represents -CH¿2?- or -CH2CH2-; Y represents -CH=, -CH2-, -CH2CH= or -CH2CH2-, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when X is -CH2- and Y is -CH= or -CH2CH=, the broken line represents a double bond; or a pharmaceutically acceptable salt thereof, are tachykinin receptor antagonists of use, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
CN103102352A Tyrosine kinase inhibitor indolinone derivative The invention belongs to the technical field of medicine, and in particular relates to a tyrosine kinase inhibitor indolinone derivative as shown in formula (I), as well as a deuterium substituent, a pharmaceutically acceptable salt or a stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, n and ring A are defined as in the specification. The invention further relates to a preparation method of the compounds, a pharmaceutic preparation containing the compounds as well as an application of the compounds for preparing medicines for preventing or treating fibrotic diseases and hyperplasias, in particular to breast cancer, colorectal cancer, non small cell lung cancer, anti-angiogenesis and/or reducing vascular permeability.
CN102813657A Composition of cefazolin sodium pentahydrate and sulbactam sodium The invention relates to a composition of cefazolin sodium pentahydrate and sulbactam sodium. Compared with the antibacterial effect of cefazolin sodium pentahydrate cefazolin sodium, the composition has excellent antibiotic activity and low resistant rates.
CN101780087A Anti-infective pharmaceutical composition containing cefminox The invention belongs to the technical field of medicines, discloses an anti-infective pharmaceutical composition containing cefminox, and relates to a preparation method of the pharmaceutical composition and an application of the medicine in preparing the medicines for treating infectious diseases. By the combination of the cefminox, Na2HPO4/NaH2PO4 and arginine, the invention solves the problem of the prior art that the cefminox is easy to hydrolyze and is unstable after storage and clinical dosage. The pharmaceutical composition has stable property, convenient storage and improved clinical medication safety.
WO2013174207A1 Protein tyrosine phosphatase inhibitor, preparation method and uses thereof Disclosed in the present invention is a protein tyrosine phosphatase inhibitor. The preparation method therefor is: extracting the crude product from the Isaria fumosorosea Wize solid or liquid fermentation broth using ethyl acetate, ethanol, methanol, or a mixed solvent of chloroform and methanol; separating the obtained extract using column chromatography on silica gel; and obtaining the target product. The inhibitor can be used to prepare pharmaceutical compositions for treating and preventing diabetes, obesity and cancers.
EP0894004B2 Method for enhancing functional recovery of motor coordination, speech or sensory perception after central nervous system ischemia or trauma The present invention provides methods and compositions for treatment of mammals afflicted with an ischemic or traumatic injury of the central nervous system. The present invention capitalizes in part upon the discovery that administration of a morphogen to such a mammal provides significant improvement in central nervous system function, even when administered after central nervous system tissue has been damaged. The methods involve the administration of dimeric proteins defined as morphogens, inducers of these morphogens, or agonists of the corresponding morphogen receptors, or implantation of cells stimulated by exposure to the morphogens. The proteins defined as morphogens comprise a structurally and functionally distinct family within the TGF-β superfamily. Osteogenic protein-1 (OP-1) is considered to be an exemplary and preferred member of this morphogen family.
US7135587 Such as 3-biphenyl-4-yl-3-(2-(3-(pyridin-2-ylamino)pro-poxycarbonylamino) -ethanoylamino)propionic acid; thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. osteoporosis, infections, restenosis Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5′, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.
US20060252747 Substitituted 1-piperidin-3-yl-piperidin 4-yl-piperazine derivatives and their use as neurokinin auantagonists This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety and depression, irritable bowel syndrom (IBS), circadian rhythm disturbances, visceral pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P, Neurokinin A and Neurokinin B by blocking the NK1, NK2 and NK3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
WO2007115975A2 USE OF kappa OPIOID RECEPTOR ANTAGONIST-CONTAINING COMPOSITIONS FOR THE TREATMENT OF DISSOCIATIVE DISORDERS The invention relates to the use of a composition comprising kappa opioid receptor antagonists for producing a drug for the treatment of dissociative disorders in humans.
CN102895649A Medicinal composition for treating liver injury and method for preparing medicinal composition for treating liver injury The invention relates to the field of medicine and discloses a medicinal composition for treating liver injury and a method for preparing the medicinal composition for treating liver injury. The medicinal composition consists of oxidized form glutathione disodium and inosine and has an obvious curative effect on liver injury.
EP2298751A2 Polymorphs of ritonavir This Application concerns the use of Form II crystalline ritonavir as a pharmaceutical agent, as well as methods of preparing pharmaceutical compositions, which methods employ Form II crystalline ritonavir. The Application further concerns methods for obtaining Form I crystalline ritonavir, which methods employ Form II crystalline ritonavir.
US8163528 Nucleic acid molecules encoding thymidine kinase fusion proteins The present invention provides isolated nucleic acid molecules encoding a Herpesviridae thymidine kinase enzyme comprising one or more mutations, at least one of the mutations encoding an amino acid substitution located toward the N-terminus from a DRH nucleoside binding site which increases a biological activity of the thymidine kinase, as compared to unmutated thymidine kinase. Such mutations include amino acid substitutions within a Q substrate binding domain which increases a biological activity of the thymidine kinase, as compared to unmutated thymidine kinase. Within a further aspect, fusion proteins are provided which have both guanylate kinase and thymidine kinase biological properties. Also provided are vectors suitable for expressing such DNA molecules, as well as methods for utilizing such vectors.
CN103099796A Propylene glycol marinate sulfate-containing sustained-release preparation and preparation method thereof The invention discloses a propylene glycol marinate sulfate sustained-release preparation and a preparation method thereof. The propylene glycol marinate sulfate sustained-release preparation comprises: propylene glycol marinate sulfate, a sustained-release skeleton matrix, a filler, a surfactant, a lubricant and a binder. The propylene glycol marinate sulfate sustained-release preparation disclosed in the invention can achieve long-acting release, and can release drug ingredients stably and evenly within 24h.
US20080226749 Administering Uncaria rhynchophylla herbal extract; granulation, spray drying, freeze drying The present invention discloses a pharmaceutical composition for inhibiting a snore symptom, which comprises medicinal material of Uncaria rhynchophylla. The above pharmaceutical composition of the present invention also comprises medicinal materials of Uncaria rhynchophylla, Ephedra, Prunus armeniaca, and Glycyrrhiza uralensis.
CN102805750A Composition of aescine derivative and salt thereof, preparation method and medical uses thereof The invention provides an aescine derivative composition and a salt thereof, and a preparation method and medicinal uses. According to the present invention, the composition belongs to a biological enzyme hydrolysis product of escin, and provides strong anti-inflammatory and anti-edema activities compared with the aescine, hemolysis safety is good, the preparation process has strong industrial production executability, and the composition can be used for developments of anti-inflammatory drugs and anti-edema drugs.
CN102010424B Crystal form III of (S)-alpha, alpha-[(2-chlorphenyl)-(4,5,6,7-thiophane[3,2-c]pyridine-5-yl)-N'-(dimethyl)methylene] acethydrazide and preparation method thereof The invention relates to a crystal form III of (S)-alpha, alpha-[(2-chlorphenyl)-(4,5,6,7-thiophane[3,2-c]pyridine-5-yl)-N'-(dimethyl)methylene] acethydrazide and a preparation method thereof, and also relates to a drug composition prepared from the new crystal form III and application thereof. The characteristics of the crystal form III are represented by powder X-ray diffraction data and melting point data.
WO2008047307A1 Pyrido [2, 3-d] pyrimidines and their use as kinase inhibitors The present invention provides derivatives of pyrido [2,3-d]pyrimidin-7-one of formula (I). These compounds are kinase inhibitors, including compounds that show antiproliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
WO2010087471A1 Hydroxypyrazinecarboxamide derivatives Provided are novel hydroxypyrazinecarboxamide derivatives which are useful in the prevention and/or treatment of blood coagulation disorders. In more detail, compounds represented by general formula (i) or pharmacologically acceptable salts thereof are provided. In general formula (i), R1 and R2 are each independently a hydrogen atom, a C1-4 alkyl group, or the like, or R1 and R2 are bonded to each other to form a C3-5 alkylene group or the like; R3 is a hydrogen atom or a C1-4 alkyl group; R4 and R5 are each independently a hydrogen atom, a C1-4 alkyl group, a C2-4 alkenyl group, or the like; R6 and R7 are each independently a hydrogen atom or a C1-4 alkyl group; X is a mono- or bi-cyclic C3-10 cycloalkyl group, a mono- or bi-cyclic C6-10 aryl group, or the like, said cycloalkyl group and aryl group being optionally substituted by 1 to 3 substituents selected from group (α) of substituents; and Y is a group having the general formula: -C(OH)Ra-, a carbonyl group, an oxygen atom, or the like.
CA2410037C 3-phenyl-imidazo-pyrimidine derivatives as ligands for gaba receptors A class of 3-phenylimidazo(1,2-a) pyrimidine derivatives (of Formula I, or salt or prodrug thereof : I) wherein Y represents a chemical bond, an oxygen atom, or a -NH- linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano trifluoromethyl, nitro, -ORa, -SRa, -SORa, -SO2Ra, -SO2NRaRb,-NRaRb, -NRaCORb, -NRaCO2Rb, -CORa, CO2Ra, -CONRaRb or -CRa=NORb; andRa and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group.), substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, are selective ligands for GABAA receptors, in particular having good affinity for the a2 and/or a3 and/or a5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
CN102552291A Vein medication preparation for fospropofol disodium, as well as preparation method and application of vein medication preparation The invention provides a vein medication preparation for fospropofol disodium, as well as the preparation method and the application of the vein medication preparation. The vein medication preparation comprises fospropofol disodium, pH buffer regulator, osmotic pressure regulator and antioxidant; and the preparation is mainly used for anesthetic in surgery. The invention has the advantages that suitable pH buffer regulator is used, the fospropofol disodium has the least degradation products at 121 DEG C through the buffered pH range, and the preparation is kept steady at room temperature.
CN103271916A Applications of Myriberine A in preparing drugs for treating prostate cancer The invention discloses applications of Myriberine A in preparing drugs for treating prostate cancer, belonging to the technical field of new applications of drugs. Detected through in-vitro MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anti-tumor activity evaluation, Myriberine A also has remarkable inhibition action on the growth of human prostate cancer cell strains ALVA, gpc-1, 9L-B and Du145. Therefore, Myriberine A can be used for preparing drugs for resisting prostate cancer, and has good development and application prospects. The applications of Myriberine A in preparing drugs for treating prostate cancer are disclosed for the first time, and the inhibitory activity to the prostate cancer is unexpectedly strong.
WO2013109201A1 Pharmaceutical compositions comprising cefprozil and clavulanic acid The present invention relates to pharmaceutical formulations comprising cefprozil and clavulanic acid to be used in the treatment of diseases caused by upper and lower respiratory tract infections, skin and soft tissue infections and urinary system infections. Said formulations are characterized in being in effervescent form.
US8101599 Pharmaceutical composition containing anti-hypertensive agents The present invention relates to a combination of organic compounds, a pharmaceutical composition and a kit of parts comprising said combination of organic compounds and to a method of treatment or prevention of certain conditions or diseases.
US20120041016 11-Aza, 11-Thia and 11-Oxa Sterol Compounds and Compositions The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
US20130035350 Novel Quinazoline Derivatives This disclosure concerns novel quinazoline compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful anticancer agents, especially in inhibiting the function of the EGF receptor tyrosine kinases, HER1 tyrosine kinase, and HER2 tyrosine kinase. Thus, the disclosure also concerns a method of treating hyperproliferative diseases or conditions, such as various cancers and benign prostate hyperplasia (BPH), by use of these novel compounds or a composition comprising such novel compounds.
WO2014050105A1 Amorphous ulipristal acetate A novel form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the ulipristal acetate are provided. An amorphous ulipristal acetate or a novel ulipristal acetate substance containing an amorphous ulipristal acetate is obtained by dissolving a raw ulipristal acetate in a halogenated hydrocarbon and condensing the solution. The amorphous ulipristal acetate may have an exothermic peak at about 135 to 145oC in a differential scanning calorimetry spectrum.
EP2763670A1 Reactivation of hiv-1 gene expression to treat persistent hiv infection The present invention provides new methods of treatment of lentivral infections, more particularly to treat latent retroviral HIV infections, present in cells of the infected subject, based on the re-activation of said viruses. The invention uses a combination therapy using several agents that result in strong re-activation of the latent HlV-virus that could destroy the infected cells and elicite an immune response in the subject. This could present further spread of the infection, with the ultimate aim to eradicate the virus completely in said subject.
EP1263742B1 Oxazolidinone thioamides with piperazine amide substituents The present invention provides a compound of formula (I) which has potent activities against gram-positive and gram-negative bacteria.
US20080103107 Screening Methods The present invention provides materials and methods relating to screening for compounds useful in the treatment of Alzheimer's disease and related conditions. In particular, screening methods using tyrosine kinases are provided, as are methods relating to the role of tyrosine kinases as therapeutic targets.
US6903081 Phosphoramidates and methods therefor Novel phosphoramidate derivatives of hydroxy functional or amino functional compounds, including amino acids, peptides, peptidomimetics and nucleotide analogs, are described. The compounds enable enhanced intracellular delivery of drugs as their corresponding phosphate esters or amides. Described phosphoramidate compounds exhibit antiproliferative activity. Pharmaceutical formulations are provided for treatment of cancers.
EP2141172A1 Cyclopropyl polymerase inhibitors Compounds of formula I: wherein: R2 is hydrogen or C1-C4alkyl; R3 and R4 are hydrogen, -C(=O)R5, or -C(=O)CHR6-NH2; or R3 is hydrogen and R4 is a monophosphate-, diphosphate-, or triphosphate ester; or R3 is hydrogen, -C(=O)CHR5, or -C(=O)CHR6-NH2 and R4 is each R5 is hydrogen, C1-C6alkyl, or C3-C7cycloalkyl; R6 is hydrogen or C1-C6alkyl; R7 is optionally substituted phenyl; naphthyl; or indolyl; R8 and R8' are hydrogen, C1-C6alkyl, benzyl; or R8 and R8' combined form C3-C7cycloalkyl; R9 is C1-C6alkyl, benzyl, or optionally substituted phenyl; provided that R2, R3 and R4 are not all hydrogen; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations with the compounds I; the use of compounds I, including the compounds of formula I wherein R2, R3 and R4 are all hydrogen, as HCV inhibitors.
WO2008024784A1 Alkylsulfonamide-substituted triazoles as matrix metalloprotease inhibitors Provided are MMP-2, MMP-3, MMP-9, MMP-12 and/or MMP-13 inhibitors having the Formula (I): wherein R2, R3, R4, R5, and Y are as defined herein, which are useful in the treatment and/or prevention of MMP mediated diseases and disorders.
WO2007009683A2 Pharmaceutical formulations of substituted pyrazoline compounds The present invention relates to the use of substituted pyrazoline compounds characterized in that the pharmaceutical formulation is in the form selected from: • An oral osmotically driven system for the release of the compound • A parenteral implant • A Multipore tablet • A Transdermal application system • A parenteral depotsystem • An oral formulation using a sweet tastemasker with a natural flavour or • A chewable formulation, preferably a chewing gum.
US20090022738 Multispecific deimmunized CD3-binders The present invention provides a cytotoxically active CD3 specific binding construct comprising a first domain specifically binding to human CD3 and an Ig-derived second binding domain. Furthermore, a nucleic acid sequence encoding a CD3 specific binding construct of the invention is provided. Further aspects of the invention are vectors and host cells comprising said nucleic acid sequence, a process for the production of the construct of the invention and composition comprising said construct. The invention also provides the use of said constructs for the preparation of pharmacutical compositions for the treatment of particular diseases, a method for the treatment of particular diseases and a kit comprising the binding construct of the invention.
WO2014034929A1 Hydromorphone hydrochloride-containing oral sustained-release pharmaceutical composition The present invention addresses the problem of providing a hydromorphone hydrochloride- or oxycodone hydrochloride hydrate-containing orally-administered sustained-release pharmaceutical composition, which exhibits a reliable main pharmacological effect and has excellent formulation stability for avoiding excessive release of the principal agent, such as alcohol resistance. A sustained-release pharmaceutical composition containing (A) hydromorphone hydrochloride or oxycodone hydrochloride hydrate, (B) hydroxypropyl methyl cellulose acetate succinate having a median diameter (D50) of 40 μm or less, (C) hydroxypropylcellulose, and (D) a sugar; the weight ratio (C)/(B) of the (B) component and (C) component contained in the composition being 11/3 to 3/11.
CN103126982A Novel veterinary medicament meglumine enrofloxacin injection and preparation method thereof The invention relates to a novel veterinary medicament meglumine enrofloxacin injection and a preparation method thereof. The preparation method specifically comprises the following steps of: putting injection water of which the temperature is 60-90 DEG C and an appropriate amount of alpha-pyrrolidone, propanediol and ethanol into a material mixing tank; adding meglumine in a gram-molecule ratio of enrofloxacin to the meglumine of 1:1, stirring, and then adding the enrofloxacin; performing temperature-maintaining reaction for 5-15 minutes during stirring to ensure that the meglumine and the enrofloxacin are subjected to chemical reaction to generate an enrofloxacin meglumine salt; adjusting the dosage of the meglumine to ensure that the pH value is 7.5-9.49, and complementing the injection water to a full amount; and performing filtration, encapsulation, sterilization, lamp inspection and bag printing to obtain the meglumine enrofloxacin injection. The content of the meglumine enrofloxacin injection can reach 0.5-10%, the pH value is between 7.5 and 9.49, and when the meglumine enrofloxacin injection is used for injecting an animal, the local irritation of an injection site can be reduced; and the meglumine enrofloxacin injection can be used by mixing with beta-lactam type medicaments, so that the meglumine enrofloxacin injection is convenient to use, and has a synergistic action and a good curative effect.
WO2006095723A1 Antiallergic drug It is intended to provide an antiallergic drug which has an excellent bioavailability and a long-lasting effect and exerts its effect when orally administered once a day. An antiallergic drug containing a fexofenadine alkyl ester or its salt which is to be orally administered once a day in a such a dose as giving from 10 to 60 mg per day of the fexofenadine alkyl ester or its salt to an adult.
US20090175844 Method of diagnosing bladder cancer Objective methods for detecting and diagnosing bladder cancer (BLC) are described herein. In one embodiment, the diagnostic method involves determining the expression level of a BLC-associated gene that discriminates between BLC cells and normal cells. The present invention further provides means for predicting and preventing bladder cancer metastasis using BLC-associated genes having unique altered expression patterns in bladder cancer cells with lymph-node metastasis. Finally, the present invention provides methods of screening for therapeutic agents useful in the treatment of bladder cancer, methods of treating bladder cancer and method for vaccinating a subject against bladder cancer. In particular, the present application provides novel human genes C2093, B5860Ns and C6055s whose expression is markedly elevated in bladder cancers. The genes and polypeptides encoded by the genes can be used, for example, in the diagnosis of bladder cancers, as target molecules for developing drugs against the disease, and for attenuating cell growth of bladder cancer.
CN101347404A Novel vaginal filling suppository and method of preparing the same The invention provides a novel vaginal plug which treats cervicitis postoperative wounds and is used for sterilizing, stopping bleeding, promoting wound healing and absorbing secretion and a preparation method thereof. The novel vaginal plug comprises bioactive glass, nano silver or chitin and active carbon fiber; when the novel vaginal plug is prepared, the active carbon fiber is firstly wrapped into a cylinder by medical non-woven fabrics, one end of the cylinder is fixed by flexible cords, the other end of the cylinder evenly adheres to mixed powder of the bioactive glass and the nano silver or the chitin; the active carbon fiber can also be wrapped into the cylinder by the medical non-woven fabrics containing the nano silver or the chitin, one end of the cylinder evenly adheres to bioactive glass powder, thus a semi-finished product is produced; the semi-finished product of a plug body is put into a package, sealed and sterilized for storage, thus a cervical plugging-typed finished product is produced; or the semi-finished product of the plug body is plugged into a propeller, put into the package with the propeller, sealed and sterilized for storage, thus a self-help type finished product is produced. The novel vaginal plug has the advantages of good clinical effect, reasonable design and simple implementation.
WO2009056886A1 Pyrimidine derivatives and their use as modulators of fgfr activity There is provided pyrimidine compounds of formula 1: or pharmaceutical salts thereof. There is al so provided processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, for exampl e in the treatment of proliferative disease such as cancer and particular ly in disease mediated by a FGFR inhibitory effect.
CN101548972A Solid pharmaceutical composition containing repaglinide The invention discloses a solid pharmaceutical composition containing repaglinide. The solid pharmaceutical composition can exist in various forms of dispersing tablets, oral disintegrating tablets and capsules and is used for curing the type 2 diabetes of which the high blood sugar cannot be effectively controlled by diet control and exercise.
US20090053321 Vaginal rinse with enhanced bacteriocidal activity There are provided vaginal rinse compositions, consisting essentially of :a) 1-20 wt % of a mucosally acceptable peroxide, b) 0.5-15 wt % of a mucosally acceptable sulfate, bisulfate, pyrosulfate salt of an inorganic cation or mixtures thereof, and c) water to 100 wt %. There are further provided methods of preparing and using said compositions as well as kits for maintaining the components to prepare said compositions.
CN103230380A Divalproex sodium enteric-coated tablet core as well as preparation method and application thereof The invention relates to a divalproex sodium enteric-coated tablet core as well as a preparation method and an application thereof. The divalproex sodium enteric-coated tablet core is used for dry granulation. The divalproex sodium enteric-coated tablet core comprises the following components: 20-70 percent of divalproex sodium, 10-70 percent of filling agent, 0.5-20 percent of disintegrating agent, 5-20 percent of antisticking agent, 0.5-10 percent of talcum powder and 0.5-5 percent of magnesium stearate, wherein the antisticking agent is selected from one or a combination of silicon dioxide, superfine silica powder and silicon dioxide precipitate. The divalproex sodium enteric-coated tablet core prepared by using the preparation method is complete in release in vitro, higher in in-vitro dissolution speed and release rate and high in quality and has better safety and safety. The dry granulation method has the advantages of simple, convenient and feasible process, low cost, easiness in mass production, environmental friendliness and the like.
US20080138357 Vaccines Against Neisseria Meningitidis Various polypeptides, or a variant or fragment thereof or a fusion of these are described which are useful in a vaccine. The polypeptide may be a polypeptide comprising the amino acid sequence selected from any one of SEQ ID Nos (2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68); or a fragment or variant thereof or a fusion of such fragment or variant, and is useful in a vaccine against Neisseira meningitidis.
US20070254868 such as 3-(1-(2,3-difluorophenyl)-1H-tetrazol-5-yl)-5-(4-(4-methylpiperazin-1-yl) phenyl)pyridin-2-amine, used as anticarcinogenic agents or for the treatment of atherosclerosis and lung fibrosis The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders.
US20120165293 Synthesis of prostanoids The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.
CA2189984C P75 tnf receptor promoters The present invention concerns a promoter sequence for the p75 tumor necrosis factor receptor, including 5' upstream and first intron promoter sequences and a first transcription inhibitory sequence, and their preparation and use.
CN101836952A Ambroxol injection and preparation method thereof The invention provides an ambroxol injection and a preparation method thereof; the injection contains ambroxol and the pharmaceutical acceptable salt thereof, disodium hydrogen phosphate and citrate, wherein the weight ratio of the ambroxol and the pharmaceutical acceptable salt thereof, the disodium hydrogen phosphate to the citrate is 1:0.18 to 0.22:0.12 to 0.16; and preferably, the weight ratio of the ambroxol and the pharmaceutical acceptable salt thereof, the disodium hydrogen phosphate to the citrate is 1:0.20:0.14. The pharmaceutical acceptable salt of the ambroxol is preferred to be hydrochloride. The used amount of active carbon adopted in the preparation is 0.2 to 0.3 percent.
WO2012138003A1 Uses of a desulfated heparin-bile acid derivative for the prevention and treatment of inflammatory diseases The present invention relates to the uses of a desulfated heparin-bile acid derivative for the prevention and treatment of inflammatory diseases. More particularly, the present invention relates to a composition for preventing and treating inflammatory diseases, which includes a heparin-bile acid derivative the anticoagulation reactive site of which is partially desulfated in order to enhance absorbability into the body and reduce the side effects thereof, to the uses of the desulfated heparin-bile acid derivative for the prevention and treatment of inflammatory diseases, and to a method for preventing and treating inflammatory diseases using the desulfated heparin-bile acid derivative. The novel desulfated heparin-bile acid derivative improves the absorption of heparin drugs into the body through the combination thereof with bile acid in order to utilize the anti-inflammatory activity of heparin, and reduces side effects such as bleeding caused by the anticoagulation activity of heparin drugs due to the partial desulfation of the heparin.
US20120258060 Methods for protecting the skin from radiation insults The present invention relates to methods and compositions for the protection of skin and mucous membranes from undesirable side effects of ionizing radiation in a patient undergoing ionizing radiation therapy. In particular, the application describes compositions and methods comprising the topical use of Nrf2 inducers.
WO2014060512A1 Fatty acid acylated amino acids for growth hormone delivery The present invention relates to growth hormone compositions comprising a fatty acid acylated amino acids (FA-aa's), which may be used in pharmaceutical compositions such as pharmaceutical compositions for oral administration of growth hormone.
EP1495758A2 Formulations and methods for treatment of mucosal associated conditions with an immune response modifier Use of an immune response modifier (IRM) compound selected from the group consisting of imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, 1,2-bridged imidazoquinoline amines, thiazolo- and oxazolo-quinolineamines and pyridinamines, imidazonaphthyridine and tetrahydroimidazonaphthyridine amines in the manufacture of a pharmaceutical formulation for the treatment of cervical dysplasia, said formulation additionally comprising: a fatty acid; a preservative system; and a carbomer.
US20080200556 Amine Compounds And Inhibiting Neurotrasmitter Reuptake The invention relates to amine compounds as well as methods and materials involved in modulating neurotransmitter reuptake. For example, the invention provides amine compounds, methods for synthesizing amine compounds, and methods for inhibiting neurotransmitter reuptake.
US20080176932 Pharmaceutical Compositions Containing Baicalein And Baicalin With Synergistic Effect In Tumor Treatment Provided is a pharmaceutical composition with synergistic anti-tumor activities, comprising baicalein and a compound of formula I, characterized in that the molar ratio of baicalein and the compound of formula I is between 1:1 and 1:4, wherein R1 represents a glucuronic acid group, and R2 represents a hydrogen or hydroxyl group. Also disclosed is the use of the composition as well as a method of its preparation.
CN102871989A External preparation containing either honokiol or pharmaceutically acceptable salt of honokiol and new application The invention belongs to the field of a medicine, and relates to a new application of either he honokiol or a pharmaceutically acceptable salt of the honokiol and an external preparation containing either honokiol or the pharmaceutically acceptable salt of honokiol. The new application is specially an application of a medicine for treating excessive keratinization and keratotic skin diseases. With the adoption of the new medicinal application, external preparation is prepared by adding common adjuvants in the pharmacy into either honokiol or the pharmaceutically acceptable salt of honokiol as a main active component or an exclusive component. According to the invention, the external preparation contains the following components by weight: 0.01% to 10% of either honokiol or the pharmaceutically acceptable salt of honokiol and 0.1% to 10% of high-efficient skin penetration enhancer. The above external preparation containing either honokiol or the pharmaceutically acceptable salt of honokiol can be utilized to implement an aim of treating the keratotic skin diseases in the way of transdermal delivery, and cutaneous penetration is obvious and an effect is remarkable, so that a new selection is provided for a clinical treatment.
US20130085114 Method for treating varicocele or male infertility using anthocyanin extracted from black soybean The present invention relates to the therapeutic or ameliorating effects of anthocyanin extracted from black soybean on varicocele or male infertility. In particular, the present invention relates to a method for treating or ameliorating varicocele or male infertility using anthocyanin extracted from black soybean.
WO2012085222A1 Novel phenazine derivatives and their use The present invention is directed to novel compounds of formula (I) and their use as anti-angiogenic agents and anti-cancer agents.
WO2007142231A1 Agent for improvement in blood fluidity The object is to develop an agent for reducing a blood viscosity which can act rapidly in a normal person having a normal daily life. Disclosed is an agent for improving a blood fluidity or for reducing a blood viscosity which comprises an orally ingestible specific amino acid composition. Also disclosed is a beverage/food comprising the agent.
EP2077845A2 Macrocyclic quinazoline derivatives as vegfr3 inhibitors The present invention relates to the use of some of the macrocyclic quinazoline derivatives described in PCT publication WO2004/105765 as inhibitors of VEGFR3 mediated biological activities, especially those activities which are mediated by VEGFR3 ligands VEGF-C and/or VEGF-D.
US6881756 Method for treating skin disorders The present invention relates to a method for reducing inflammation in the skin and/or treating inflammatory skin disorders, pain, or pruritis by topically applying a composition comprising totarol or a pharmaceutically-acceptable ester thereof.
CN103585142A Medicine composition containing docetaxel The invention belongs to the technical field of medicines, and discloses a medicine composition containing docetaxel. The medicine composition comprises the docetaxel, anhydrous ethanol, anhydrous citric acid and Tween 80, wherein the water content of the docetaxel, the water content of the citric acid, the C2H60 content of the ethanol and the oleic acid content and other fatty acid content of the Tween 80 have important effects on the mass of a docetaxel preparation. The medicine composition adopted by the invention reduces the content of impurities in products; in particular, after the medicine composition is compatible with normal saline through the stability experiment, the content of impurities E is prominently lower than that of a contrast group.
US20080038355 Bioadhesive dosage form of steroids Bioadhesive steroid nanoparticles are used to prepare a rapidly disintegrating solid oral dosage form of steroid. The bioadhesive steroid nanoparticles have a bioadhesive polymer surrounding the steroid nanoparticles and with an average diameter of less than 1000 nm. Hence, the solid oral dosage form, containing the bioadhesive steroid nanoparticles, a disintegrant and an effervescent agent, instantly disintegrates in the oral cavity and adheres on the periodontal pocket and oral mucosa to release steroid rapidly.
CN1562020A Corydalis B powder injection and its preparing method A powder injection of corydalis B for treating the pain, headache and insomnia caused by intenal diseases, menalgia, etc contains corydalis B and pharmacological acceptable auxiliaries.
US20100137368 Pyridine derivatives as fast dissociating dopamine 2 receptor antagonists The present invention relates to (1-benzyl-piperidin-4-yl)-(pyridin-2-yl)-amines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
US7232846 endogenic polyamines (putrescine, spermidine, spermine), 1,3-propanediamine, their salts and solvates, bioprecursor amides for therapeutical and prophylactic treatment of alcoholism in a human The oral administration to genetically alcoholic rats (from the strain UChB of the University of Chile) of a compound selected from endogenic polyamines (putrescine, spermidine, spermine), 1,3-propanediamine, their pharmaceutically acceptable salts and solvates, and their bioprecursor amides, causes a significant reduction in the alcohol consumption. The activity lasts for some time after the treatment period. Besides, there is a virtually null disulfiram-like adverse effect, what constitutes an advantage over the unpleasant use of some anti-alcoholism agents, such as calcium cyanamide or disulfiram itself. Therefore, the compounds of the invention are useful for the preparation of medicaments for the therapeutic and/or prophylactic treatment of alcoholism in human beings.
US7211680 (5Z,7E,22E)-(1S,3R,24R)-25-phenyl-26,27-cyclo-9,10-secocholesta-5,7,10(19),22-tetraene-1,3,24-triol; treating hyperprolifierative diseases of the skin, tumor diseases and precancerous stages, auto-immune diseases, rejection reactions in the case of autologous, allogenic or xenogenic transplants, AIDS Compounds of Formula I, wherein Y1, Y2, R1–R6, Q and Z are as defined herein, are vitamin D derivatives. These compounds are useful for, e.g., the treatment hyperprolifierative diseases of the skin, tumor diseases and precancerous stages, auto-immune diseases, rejection reactions in the case of autologous, allogenic or xenogenic transplants, AIDS, atopic skin conditions, secondary hyperparathyroidism, renal osteodystrophia, senile and postmenopausal osteoporosis, diabetes mellitus type II, degenerative diseases of the peripheral and central nervous system, hypercalcemias, granulomatous diseases, paraneoplastic hypercalcemias, hypercalcemias in hyperparathyroidism, hirsutism, ateriosclerosis, and/or inflammatory diseases.
US20070213381 Topical Compositions Comprising Telmesteine for Treating Dermatological Disorders This invention relates to topical compositions, such as creams and lotions, that comprise or consist essentially of Telmesteine, or a pharmaceutically acceptable salt thereof, as the active ingredient, and methods for their use in treating a variety of dermatological diseases and disorders, including atopic, dermatitis (eczema), allergic contact dermatitis, seborrheic dermatitis, radiation dermatitis, psoriasis, xerosis and atopy.
US20120232124 Compositions and methods for prognosis and treatment of prostate cancer Described herein are compositions and methods for prognosis and treatment of prostate cancer patients. Specifically the invention relates to microRNA molecules associated with the prognosis of prostate cancer, as well as various nucleic acid molecules relating thereto or derived therefrom.
WO2014058114A1 Composition, containing cis-cyclo(l-leu-l-pro) or cis-cyclo(l-phe-l-pro), for use as an antimicrobial and antiviral agent, and preparation method therefor The present invention provides an antimicrobial composition containing cis-cyclo(L-Leu-L-Pro) as an active ingredient and having specific antimicrobial activity against the genus Streptococcus or bacteria of the genus Shigella, a pesticide composition, and a method for producing an antimicrobial agent. The present invention exhibits excellent antimicrobial activity against the genus Streptococcus or Shigella and thus can be applied to various industrial fields requiring the removal and prevention of the genus Streptococcus or Shigella bacteria. In particular, the present invention is economically advantageous in terms of the use thereof because even a small amount thereof exhibits antimicrobial activity. In addition, the present invention provides an antiviral composition containing cis-cyclo(L-Leu-L-Pro) or cis-cyclo(L-Phe-L-Pro).
US20090215819 Anti-infective and immunomodulatory compounds The present invention provides pharmaceutical compositions and methods that include the use of anti-infective compounds that potentiate the host-immune response or limit or prevent the expression or activity of individual virulence factors. In addition, the compositions have immunomodulatory activity, and therefore can be used to prime host defenses to prevent or limit bacterial, fungal, and viral viability. In the compositions and methods of the inventions, specific steps of the bacterial-, fungal-, or viral-host interaction are targeted to prevent pathogenesis (e.g., infection). Such an approach should prevent pathogenic organisms from acquiring resistance to the protective anti-infective compounds.
CN103417527A Medical uses of methyl (E)-3-[2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-2,3-dihydro-1-benzofuran-5-yl]-prop-2-enoate The invention belongs to the fields of chemical industry and medicine, and relates to medical uses of methyl (E)-3-[2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-2,3-dihydro-1-benzofuran-5-yl]-prop-2-enoate (hereafter referred to as H4 for short). The invention provides applications of H4 in preparation of antitumor drugs and a corresponding antitumor drug composition. The invention also provides a method for inhibiting tumor cell proliferation in vitro. According to the method, the H4 is added into nutrient solution of tumor cells, which include hepatoma cells, gastric cancer cells, or leukemia cells. The H4 is a natural product with small toxic side effects, high bioavailability and stable properties, and thus is valuable for clinical use. The small molecule provided by the invention is developed as a novel antitumor drug or an auxiliary component thereof, has a significant antitumor effect, and is environmentally friendly.
WO2011138512A1 Sulphated hyaluronic acid in combination with g-csf for use in mobilising blood stem cells The present invention relates to a combination of a hyaluronan oligomer and/or polymer and a factor capable of mobilizing stem cells. The present invention relates also to a use of the combination to alter the relative amounts of blood cells and/or the types of blood cells in a subject. Further, the present invention relates to a use of the combination to mobilize stem cells to the bloodstream of a subject. Additionally, the present invention relates to a hyaluronan oligomer and/or polymer.
EP1274398B1 Methods for thepreparation of effervescent granules Disclosed here are effervescent granules having a controllable rate of effervescence. In some embodiments, the such granules comprise an acidic agent, an alkaline agent, a pharmacologically active agent, hot-melt extrudable binder capable of forming a eutectic mixture with the acidic agent and, optionally, a plasticizer. The effervescent granules are made by a hot-melt extrusion process. The present invention also provides a thermal heat process for preparing a pharmacologically active agent containing effervescent granule. In certain aspects, the granules contain pharmacologically active agents such as narcotics, antidiarrheal agents, antiviral agents, anxiolytic agents, a cholesterol lowering agent, an alpha adrenergic blocking agent, a phenanthrene derivative. By way of example, some of the narcotics that may be included in the granules and in the process of preparing the granules include, by way of example: phenanthrene derivatives (e.g., morphine sulfate), and morphine derivatives (e.g., hydromorphone hydrochloride).
US20110027398 Methods of making olive juice extracts containing reduced solids Solids, including fibers can be easily removed from olive juice by mixing the olive juice with a water-miscible solvent to form two phases and separating the phases. Preferably the solvent is ethanol.
EP2564852A1 Anti-brain-tumor drug A drug containing a metal-salen complex compound which is effective for a brain tumor is provided. The present invention is an anti-brain-tumor drug containing a metal-salen complex compound represented by the following Chemical Formula (I). In the formula, M represents a metal atom which is Fe, Cr, Mn, Co, Ni, Mo, Ru, Rh, Pd, W, Re, Os, Ir, Pt, Nd, Sm, Eu, or Gd, and X represents a halogen atom.
US20120328696 Anti-parkinsonian compound acetylsalicylic acid maltol ester The present application describes a composition comprising a neuroprotective effective amount of an antioxidant acetylsalicylic acid maltol ester (AME).
US20100021570 Smoking Cessation Treatment By Reducing Nicotine Cravings, Apetite Suppression, And Altering The Perceived Taste Of Tobacco Smoke A multi-component compound for the simultaneous treatment of nicotine addiction and the side effects of nicotine withdrawal, such as excessive appetite. The first component is a bivalent negative sulfur compound in an amount effective to control nicotine craving or the withdrawal symptoms resulting from nicotine withdrawal. The bivalent negative sulfur is selected from a group that includes, but is not limited to, alkyl sulfides, colloidal sulfur, hydropersulfides, organic thio compounds or their salts. The second component is a serotonin precursor, such as tryptophan or its derivative 5-HTP, which is used to assist the body in producing more serotonin which in turn suppresses appetite. The appetite suppressant(s) are combined with the bivalent negative sulfur compound(s) to provide a single compound that reduces nicotine craving and simultaneously suppresses increased appetite resulting from nicotine withdrawal. The compound alters the perceived taste of tobacco smoke such that it is no longer enjoyable.
EP1688410A1 Crystal of phenylalanine derivative and process for producing the same The present invention provides crystals of phenylalanine derivatives of the formula (I), and particularly α -type, γ-type, ε-type, η -type, and θ -type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on the industrial scale.
US20080221180 Thiazole Derivatives and Use Thereof The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
US20050107474 Pharmaceutical compositions for the treatment of infections of the respiratory system by pathogenic agents The present invention relates to pharmaceutical compositions for the treatment of infections by pathogen agents of the respiratory system, for example Staphylococcus aureus, and more particularly it relates to the aforesaid compositions containing N-acetyl-cysteine possibly combined with thiamphenicol.
WO2014092175A1 Specific polyphenol used in food and drink products, supplements, pharmaceuticals, and the like and method for manufacturing said specific polyphenol The present invention addresses the problem of providing a method for manufacturing a comparatively high-purity ≥4-mer polyphenol by precisely isolating said ≥4-mer polyphenol from a polyphenol mixture. This method for manufacturing a specific polyphenol uses a non-acid-containing eluent to isolate a ≥4-mer polyphenol from a polyphenol mixture via gel filtration fractionation, e.g. liquid chromatography or gel filtration chromatography.
CN101759686A Synthesizing method and application of 2-substituted aryl-1-substituted benzyl benzimidazole compound The invention discloses a synthesizing method of a 2-substituted aryl-1-substituted benzyl benzimidazole compound, comprising the following steps of: adding an o-phenylenediamine compound to a reactor; adding a water-alcohol mixed solvent with 30-100 times by weight of the o-phenylenediamine compound under the stirring; then adding aromatic aldehyde, wherein the mole ratio of the o-phenylenediamine compound to the aromatic aldehyde is 1 to 2.0-2.5; then heating, refluxing and then adding a weed acid catalyst after relfuxing; continuously relfuxing and reacting for 30-90 minutes, finishing reaction; and then pouring a reaction mixture into ice water to sequentially perform stirring, pumping filtration, washing and alcohol recrystallization so as to obtain the 2-substituted aryl-1-substituted benzyl benzimidazole compound. The synthesizing method has short synthetic route, high yield coefficient, simple and moderate reaction condition, easy operation, high atom utility ratio, easy recycling of a reaction solvent in a water-alcohol system, low cost and easy obtaining of the catalyst; the whole reaction process reflects a green synthetic chemistry idea; and in addition, the obtained 2-substituted aryl-1-substituted benzyl benzimidazole compound has higher inhibitor for a thioformamide peptidase.
CN1814300A Glinide drug adjuvant composition and method for preparing drug containing same This invention discloses an auxiliary materials compound that can increase glinide type blood sugar reducing medicine dissolution. Blood sugar reducing main medicine and other auxiliary material are pulverized and through 100 items sift; the main medicine is mixed with pulverulent (slight crystals) cellulose P290, slight crystal cellulose 102, crosslinking carboxymethyl cellulose natrium as equal quantity increasing rules. soft wood is made by 2.5% polyvidone K30 water solution, then wet particle is made by through 24 items sift, then baked for 4-5 hours at 70 degree centigrade. Moister of the particles is maintained about 4%, then particles is picked up after baking and though 24 items sift, finally pharmaceutics is got after added magnesium stearate and crosslinking carboxymethyl cellulose natrium and mixed. The pharmaceutics got in this invention is stable, dissolution is high. Its long time using effect is good, security is high, price is low, adverse reaction is small, tolerance is good.
WO2009129531A2 Bupivacaine formulation in a polyorthoester carrier Effective treatments of pain, such as chronic pelvic pain, for extended periods of time are provided. The treatments include the administration of one or more drug depots intraspinally wherein the drug depots include an effective amount of bupivacaine formulated within a polyorthoester. By administration of one or more drug depots, one can relieve pain caused by diverse sources, including but not limited to chronic pelvic pain syndromes, spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discongenic back pain and joint pain, as well as pain that is incidental to surgery. In some embodiments, the relief can be for at least thirty days, at least sixty days, at least one hundred days or at least one hundred and thirty-five days.
WO2010005765A1 Method of treatment and pharmaceutical compositions The present invention relates to methods, uses, and compositions comprising the caspase inhibitor (R)-N-((2S,3S)-2-(fIuoromethyl)-2-hydroxy-5-oxo-tetrahydrofuran- 3-yl)-5-isopropyl-3-(isoqυinolin-1 -yl)-4,5-dihydroisoxazo!e-5-carboxamide, or a pharmaceutically acceptable salt thereof.
CN102863627A Cisplatin complex and preparation method thereof The invention provides a cisplatin complex which is formed by complexing cisplatin with polymer with a structure as a formula (I), and further provides a preparation method of the cisplatin complex. The cisplatin and the polymer with the structure as the formula (I) are in complex reaction in aqueous media to generate the cisplatin complex. The cisplatin complex has fine biocompatibility and is degradable, and polyethylene glycol is grafted on a side chain of the polymer, so that the prepared cisplatin complex has fine dissolvability. When the cisplatin complex is dissolved in the aqueous media, the cisplatin is protected by a hydrophilic polyethylene glycol chain segment and a hydrophobic amino acid chain segment, and accordingly sudden release of cisplatin caused by influences of a blood circulation system after intravenous injection can be effectively avoided, and stability of the cisplatin complex is improved. In addition, carboxyl contained in the cisplatin complex has pH sensitivity and deprotonation tendency in a low-pH environment, medicine release is facilitated, and medicine curative effect can be improved.
US20100137235 Methods for Concomitant Administration of Colchicine and Macrolide Antibiotics Methods for concomitant administration of colchicine together with one or more macrolide antibiotics, e.g., clarithromycin, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits.
CN101022853A Mixture of catechins or polyphenols extracted from chinese green tea or other vegetables for the prevention of prostate cancer and for the treatment of prostate hypertrophy (BPH) The formulation and modality of use of a pharmaceutical preparation having the properties described below is described. This preparation is a product that has proven to be efficacious in the chemical prevention of prostate cancer in a clinical pilot study when administered in adequate systemic dosage without the aid of other conventional drugs or remedies and without adverse effects in a group of subjects at risk of development of the illness. The same reduction of the preparation proved efficacious in symptomatology of benign prostate hypertrophy and especially as concerns the difficulty of urination when administered in adequate dosage systemically without the aid of other drugs or conventional remedies and without adverse effects in the patients subject of the study.
WO2011054885A1 1-substituted 2-azabicyclo [3.1.1] heptyl derivatives useful as nicotinic acetylcholine receptor modulators for treating neurologic disorders This invention provides 2-azabicyclo[3.1.1]heptyl derivatives, and methods for producing them, which are useful therapeutic agents for preventing or treating central nervous system disorders and disease mediated by a Nicotinic Acetylcholine Receptor such as, but not limited to, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy, dementia, pain and nicotine addiction.
US20140047569 Methods of Treating Disorders Associated with Protein Aggregation The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.
CA2261706C The use of growth factor modulating compounds The invention relates to the use of a compound containing a high density, negatively charged domain of vicinally oriented radicals for the preparing of a medicament providing a growth factor modulating activity in mammals including man.
CA2210891C Valaciclovir tablets containing colloidal silicon dioxide A tablet comprising of at least 50 % w/w valaciclovir, and 0.05 to 3 % w/w colloidal silicon dioxide is provided which has excellent hardness and friability properties while still maintaining good lubrication of the tablet granules.
US7345067 peroxisome proliferator activators such as (2-methyl-4-{methyl-[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethyl]-amino}-phenoxy)-acetic acid, used as lipid modulators and insulin sensitizers This invention relates to compounds of the formula wherein X is N and Y is S or O; or X is S or O and Y is N; R1 is hydrogen or C1-7-alkyl; R2 and R3 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl and C1-7-alkoxy; R4, R5, R6, and R7 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halogen, C1-7-alkoxy, C1-7-alkyl-C1-7-alkoxy-C1-7-alkyl, C2-7-alkenyl, C2-7-alkinyl, fluoro-C1-7-alkyl and cyano; R8 is selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R9 is selected from the group consisting of hydrogen, C1-7-alkyl, C2-7-alkinyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R10 is selected from the group consisting of hydrogen, C1-7-alkyl, C2-7-alkinyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R11 is aryl or heteroaryl; N is 0, 1 or 2; and all enantiomers and pharmaceutically acceptable salts and/or esters thereof and their use as PPAR activators.
CN101450911B Benzoic acid derivates substituted by adamantane The invention belongs to the technical field of medicine, in particular to adamantane substituted benzoic acid derivatives shown in the general formula (I), pharmaceutically acceptable salts or isomers thereof, wherein R<1>, R<2>, R<3>, R<4>, R<5>and n are defined as the description. The invention also relates to a method for preparing the compounds, medical compositions containing the compounds,and application of the compounds in preparing medicines for treating and/or preventing infectious disease.
WO2012142474A3 N-acetyl beta alanine methods of use Methods for increasing athletic performance, preventing paresthesia, increasing beta alanine absorption and cell membrane permeability through both passive diffusion and active transport, and increasing the half-life of beta alanine present in a blood stream in a human or animal are disclosed. Each method includes administering to the human or animal a pharmaceutically effective amount of N-Acetyl Beta Alanine or an N-Acetyl Beta Alanine composition.
CN101693076A Content measuring method of vitexin in tropaeolum heat-clearing granules The invention relates to a content measuring method of vitexin in tropaeolum heat-clearing granules, which is realized by adopting a high performance liquid chromatography. The content measuring method has simple operation, accurate results, high sensitivity, good reproduction quality, good recovery rate, small interference and no interference for measuring a negative contrast solution, and can be used as an effective method for controlling the internal quality of the tropaeolum heat-clearing granules.
CN103142537A Calcitriol slow-release preparation troche The invention relates to a calcitriol slow-release preparation troche which comprises a core and a coating, wherein the core is an aggregate sheet which comprises calcitriol, hydroxypropyl methylcellulose, lactose, magnesium stearate, talcum powder and 95% ethanol solution; and the coating comprises a slow release coating material, polyethylene glycol and calcitriol. According to the preparation, the dosing time is reduced, the compliance of the patient is improved, the side effect caused by overhigh peak concentration is reduced, and the effective blood concentration for longer time is maintained.
WO2005027923A1 Use of vitamin d3 analogue for the treatment of benign prostatic hyperplasia The use of 1-alpha-fluoro-25-hydroxy-16,23E-diene-26,27-bishomo-20-epi cholecalciferol, or a pharmaceutically acceptable salt or ester thereof, for the manufacture of a medicament for the prevention and/or treatment of benign prostatic hyperplasia (BPH) and associated symptoms.
US6969719 Such as 3-((3-bromo-4-hydroxyphenyl)methyl)-5-ethyl-7,8-dihydro-2-(tetrahydro-2H -pyran-4-yl)amino)-3H-imidazo(2,1-b) purin-4(5H)-one for treating sexual disorders A polycyclic guanine phosphodiesterase V inhibitor having the formula (I.1) or (II.1), with the variables defined herein, which is useful for treating sexual dysfunction and other physiological disorders: A representative example is:
US20090227688 Admixture of carotenoids having provitamin a activity and carotenoids devoid of provitamin a activity for treating aging symptoms Intimate admixtures of at least one carotenoid having provitamin A activity and at least one carotenoid devoid of provitamin A activity are well suited for treating the undesirable cutaneous signs of skin aging, in particular the determination of the skin and/or of the mucous membranes by inhibiting the activity and/or the expression of collagenases and by increasing the synthesis of collagen.
WO2007148780A1 6-(heterocycle-substituted benzyl)-4-oxoquinoline compound and use of the same as hiv integrase inhibitor A compound represented by the general formula [I], a pharmaceutically acceptable salt thereof, or a solvate of the compound or the salt; and a pharmaceutical composition, an anti-HIV agent, and an HIV integrase inhibitor, each comprising the compound. [I] wherein each symbol is as defined in the description. The compound has an action of inhibiting the HIV integrase activity, and therefore is useful as an anti-HIV agent or a therapeutic or prophylactic agent for AIDS. By using in combination with other anti-HIV agent such as a protease inhibitor and a reverse transcriptase inhibitor, the compound can act as a more effective anti-HIV agent. Further, because of its high inhibitory activity specifically against an integrase, the compound can act as an agent which is safe for a human body and has few adverse side-effects.
CN101961334A Combined drug of pantoprazole and domperidone The invention provides a combined drug of pantoprazole and domperidone and in particular provides application of pantoprazole and domperidone to preparing combined injections for treating gastric ulcer, duodenal ulcer, gastro-esophageal reflux diseases or functional dyspepsia. The invention also provides the combined injections for treating gastric ulcer, duodenal ulcer, gastro-esophageal reflux diseases or functional dyspepsia, including different specifications of unit preparations, pantoprazole and domperidone for simultaneous, respective or successive administration and preparations prepared by pharmaceutically acceptable vectors. The weight ratio of pantoprazole and domperidone is 1:1-5:1, and the pantoprazole and domperidone contain excipients, stabilizing agents, etc. Through combined injection administration, the invention improves the bioavailability of pantoprazole and domperidone and ensures the treatment effects to be obviously better.
CN103040855A Pharmaceutical composition of fludarabine phosphate and preparation method thereof The invention relates to fludarabine phosphate, in particular to a pharmaceutical composition of fludarabine phosphate. The pharmaceutical composition comprises fludarabine phosphate, sodium chloride and excipient in weight ratio of 10: (1-5): (6-12) and preferably 10: (1-3): (6-10). The excipient is selected from at least one type of mannite, glucose, dextran, sorbitol and lactose, and preferably mannite or sorbitol. The pharmaceutical composition of fludarabine phosphate has low impurity content, is highly stable, and is suitable for clinical application.
CN103222957A Strychnine-beta-cyclodextrin polymer liposome, preparation method and applications thereof The present invention discloses a strychnine-beta-cyclodextrin polymer liposome, which contains, by weight, 0.5-2 parts of strychnine, 10-20 parts of a strychnine-beta-cyclodextrin polymer inclusion compound, 40-200 parts of lecithin, 5-20 parts of cholesterol, and 0.5-20 parts of carbomer. The present invention further discloses a strychnine-beta-cyclodextrin polymer liposome preparation method, which comprises: carrying out inclusion on strychnine with a beta-cyclodextrin polymer to obtain an inclusion compound, and then preparing the liposome. According to the present invention, the strychnine is encapsulated into the cavity of the beta-cyclodextrin polymer and the bilayer of the liposome so as to improve drug loading capacity, prolong an elimination half-life of the strychnine, improve stability, achieve targeting of the inclusion compound in the lymphatic system, reduce toxic and side effects on heart and central nervous system, and improve bioavailability.
CN102652749A Application of 2-cycloxyl substituted or cyclothio substituted hydroxyacetophenone in treatment of metabolic disease The invention discloses an application of 2-cycloxyl substituted or cyclothio substituted hydroxyacetophenone in treatment of metabolic diseases. In particular, the invention relates to an application of a compound as shown in general formula (I) in preparation of medicaments for preventing or treating metabolic diseases. Wherein X is selected from H, NO2, or OH; Y is selected from H or OH; Z is selected from O or S; A ring is selected from an alicyclic group, a heteroalicyclic group, an aryl, and a heteroaryl; Z and R can be connected with any appropriate connection site on the A ring; R represents one or more than one substituent. The metabolic diseases comprise metabolic syndrome, obesity, diabetes mellitus, hyperglycemia, diabetic nephropathy, hyperlipidemia, hypertension, coronary heart diseases, atherosclerotic cardiovascular diseases, cardio-cerebrovascular diseases, and diseases of the liver, the kidney, and the thyroid as a result of the above.
WO2005054252A1 Crystal of hydrochloride of sulfoxide derivative Novel crystal of a hydrochloride of sulfoxide derivative that is useful as a neurokinin receptor antagonist.
WO2009016329A1 Use of gabaa receptor antagonists to treat cognitive impairment in patients with psychiatric conditions The present invention relates to the treatment of impaired cognitive function in patients with psychiatric conditions such as schizophrenia with inhibitors of Ϝ-aminobutyric acid (GABA) neurotransmission, such as flumazenil. Methods of treatment and uses of blockers of inhibitory GABA neurotransmission are provided, along with screening methods for identifying further therapeutic agents.
WO2006043710A1 Drug development target protein and target gene, and method of screening A novel drug development target protein and gene, and, using these, means for developing a novel pharmaceutical. In particular, there are provided an NCS protein and a gene therefor; a method of screening a drug (for example, anti-central neurologic disease agent); a regulator of diseases (for example, central neurologic disease); a process for producing drug derivatives; a complex containing a drug and an NCS protein, and a process for producing the same; a kit including a drug or its salt; a method of determining the development or development risk of given disease, a method of determining the sensitivity to drugs, and a determination kit for use in the methods; etc. Further, there is provided a compound, or its salt, capable of binding to NCS proteins, represented by the following formula (I), and provided a therapeutic or preventive agent for dementia comprising the compound of the formula (I) or pharmaceutically acceptable salt thereof as an active ingredient. (wherein R1-R8 represent hydrogen atoms, etc.)
WO2007029730A1 Amino acid composition for prevention or treatment of senile anemia Anemia often occurs with aging. Thus, the first object is to develop an effective therapeutic agent for prevention of senile anemia. An elderly population is growing toward the future. Thus, the second object is to provide an inexpensive, effective anti-aging agent which produces little adverse side effect. It is found for the first time that a preparation comprising, as an active ingredient, an amino acid composition comprising at least isoleucine (Ile), tryptophan (Trp), threonine (Thr), valine (Val), histidine (His), phenylalanine (Phe), methionine (Met), lysine (Lys) and leucine (Leu) is capable of ameliorating and recovering senile anemia, and a senile anemia-treating agent, a senile anemia-preventive agent, a cell senescence-preventive agent, a muscle anabolism-promoting agent and a muscle catabolism-preventive agent can be provided. An example of the amino acid composition comprises aspartic acid (Asp), alanine (Ala), arginine (Arg), isoleucine (Ile), glycine (Gly), glutamic acid (Glu), serine (Ser), tyrosine (Tyr), tryptophan (Trp), threonine (Thr), valine (Val), histidine (His), phenylalanine (Phe), proline (Pro), methionine (Met), lysine (Lys) and leucine (Leu).
CA2253211C Sulfonamide-substituted fused 5-membered ring compounds, their use as a medicament, and pharmaceutical preparations comprising them Compounds of the formula I (see formula I) having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastro-intestinal region or for the treatment of diarrheal illnesses.
CN1986546A Geldanamycin derivative and its preparing method and use The present invention relates to the compound as shown and its pharmaceutically acceptable salt. The present invention also relates to the preparation process and pharmaceutical use of the compound. The compound of the present invention is prepared through pseudostreptoverticillium fermentation, and experiment shows that the compound may be used in preparing cell cycle inhibitor and antitumor preparation.
CN101355934A Transcription set modifier and application of chemotherapeutics or actinotheraphy against cancer The invention relates to the use of transcriptome-modifying agents in order to prevent malignant cells from undergoing the necessary genetic changes in order to combat cell insult and survive chemotherapy or radiotherapy. Said combination of transcriptome-modifying agents comprises agents that inhibit the DNA methylation machinery plus a substance that inhibits histone deacetylation. The invention relates to a treatment kit which involves the administration of an effective dose of hydralazine and valproic acid or a salt of same in the case of magnesium valproate, which is intended for use with radiotherapy or chemotherapy in the treatment of patients cancer.
CN102805732A Tanshinone IIA lipid microsphere preparation and preparation method thereof The invention relates to a tanshinone IIA lipid microsphere preparation and a preparation method thereof. 1000 ml of the preparation is prepared according to a formula, wherein the formula comprises, by weight, 0.01-1.0 g of tanshinone IIA, 10-200.0 g of oil for injection, 2.0-20 g of an emulsifying agent, 4.0-10.0 g of an isotonic regulator and the balance of water. According to the preparation method, a drug and phospholipid are firstly dissolved in a suitable solvent, then the solvent is removed, and the resulting material is added to an oil phase, wherein entrapment rate of the prepared product is significantly improved, a disadvantages of poor water solubility of the tanshinone IIA is overcome with the preparation method, a lipid microsphere preparation with characteristics of low toxic reaction, low irritation, long effect time, sustaining and targeting is provided, a process is simple process, cost is low, and the method is applicable for industrial production.
US20070185126 Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing Them The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5 R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
US20090280143 Genetic adjuvants for immunotherapy The present invention pertains to methods and pharmaceutical compositions for modulating an immune response. The method of the present invention involves administration of an effective amount of nucleic acid molecules encoding interleukin-12 (IL-12), interferon-gamma (IFN-γ), or a combination thereof, to a patient in need of such treatment. The pharmaceutical compositions of the invention contain nucleic acid molecules encoding IL-12 and/or IFN-γ and an operably-linked promoter sequence. In another aspect, the present invention concerns expression vectors containing a nucleotide sequence encoding IL-12 and IFN-γ, and an operably-linked promoter sequence. In another aspect, the present invention concerns cells genetically modified with a nucleotide sequence encoding IL-12 and IFN-γ.
US20100256178 Super-oxide dismutase mimetics The present invention relates to compounds which are effective as catalysts for dismutating superoxide and, more particularly, the manganese or iron complexes of substituted, unsaturated heterocyclic 16-membered macrocyclic complexes that catalytically dismutate superoxide. It also relates to methods of using these complexes to reduce the concentration or the effects of superoxide, pharmaceutical compositions comprising these compounds or their metal complexes, and methods of treating conditions associated with excessive superoxide activity.
US20120115939 Methods for using lipoic acid The present provides methods for using lipoic acid. In one embodiment, the methods include administering lipoic acid to a female subject in need thereof, wherein at least 10 milligrams lipoic acid per kilogram of body weight is administered. In another embodiment, the methods include administering to a female subject in need thereof an effective amount of lipoic acid, wherein concentration of progesterone in the blood of the subject is increased compared to the subject prior to administration of the lipoic acid. The subject may be pregnant.
US20100240621 Topical pharmaceutical composition for the combination of fusidic acid and a corticosteroid The present invention relates to topical pharmaceutical compositions comprising fusidic acid and a corticosteroid. More particularly, the present invention relates to topical pharmaceutical compositions comprising fusidic acid and mometasone or halobetasol or their esters, processes for preparing the same, and the use of such compositions for prevention and treatment of dermal infections.
WO2009062402A1 Quinazolinone derivatives, the preparation methods and uses thereof The quinzolinone derivatives, the preparation methods and uses thereof. The quinzolinone compounds having the structure of general formula (I), or their pharmaceutical acceptable salts. Most of these compounds have strong activities of inhibiting PDE5, and have highly selectivity of PDE 6 which is distributed on the retina. So the present compounds are expected to exhibit good safety and effectiveness and have broad uses in clinic.
CN101390865A Anticancer composition containing lurtolecan Disclosed is an anticancer combination which is sustainable-release injection and contains lurtoteca. The anticancer sustainable-release injection contains sustainable-release microspheres and solvent; wherein, the microsphere is composed of PI3Ki and/or topoisomerase inhibitor, and sustained-release auxiliary material; the solvent is common solvent or special solvent which contains suspending agent; the viscosity of the suspending agent is 100cp-3000cp(20 DEG C-30 DEG C); the suspending agent is selected from sodium carboxymethyl cellulose and the like; the sustained-release auxiliary material is selected from polyphosphate ester copolymer such as p(LAEG-EOP),p(DAPG-EOP),p(BHET-EOP/TC),p(BHET-EOP/TC), p(BHDPT-EOP/TC), p( BHDPT-EOP/TC), p(CHDM-HOP)or p(CHDM-EOP), or the copolymer or mixture of polyphosphate ester and the followings, polylactic acid, polifeprosan, the copolymer of sebacic acid double fatty acid, poly (erucic acid dimer sebacic acid) or poly(fumaric acid sebacic acid); the anticancer combination also can be made into sustained-release implants which can be injected or implanted in tumor or the periphery of tumor with the effective medicine concentration maintained for more than 40 days; meanwhile, the systemic reaction of the medicine is obviously reduced; the treatment effects of the non-operative treatments such as chemotherapy or radiation treatment are selectively enhanced.
CN101422447A Instant film preparation containing phenylephrine hydrochloride The present invention provides a membrane preparation which is combined with phenylephrine hydrochloride, hydroxypropyl cellulose and/or hydroxypropyl methyl cellulose and can be quickly dissolved in oral cavity. The rapidly soluble membrane preparation 1 comprising phenylephrine hydrochloride 1 according to the invention is characterized by comprising a resin film 3, one layer or more than two layers of shielding layer 5, and one layer or more than two layers of medicine-containing layer 7. The shielding layer 5 is formed on the resin film 3 and comprises edible macromolecular substance and does not contain phenylephrine hydrochloride. Additionally the medicine-containing layer 7 is formed on the shielding layer 5 and comprises at least one component selected from hydroxypropyl cellulose and hydroxypropyl methyl cellulose. Furthermore the rapidly soluble membrane preparation 1 comprising phenylephrine hydrochloride 1 according to the invention can comprise one layer or more than two layers of shielding layer 5 that comprises edible macromolecular substance and does not contain phenylephrine hydrochloride according to expectation.
CA2338000C Water-soluble 4-thio-maleimido derivatives and methods for their production The present invention provides water-soluble drugs of the formula, (see above formula) in particular, a water-soluble analogues of geldanamycin, and compositions comprising the same. This invention also provides a method of rendering water-insoluble drugs soluble in water through derivatization with a bifunctional linking molecule and subsequent conjugation to a polar moiety through a thio ether. The present invention further provides use of the compounds to treat cancer that expresses heat shock protein 90 (Hsp90) in a mammal.
US20080125408 (5-propyl-2-oxo-1,3-dioxol-4-yl)methyl (5R,6S)-6-[(1R)-1-hydroxyethyl]-7-oxo-3-[[(1R,3S)-tetrahydro-1-oxido-3-thienyl]thio]-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate for teating bacterial infections such as bronchitis, sinusitis, otitis media, brain abscess, pneumonia etc; oral bioavailability The invention relates to prodrugs of sulopenem of formula (I): wherein R1 is —(C2-C8)alkyl, or a solvate or hydrate thereof. The invention also relates to the preparation, formulation, and use of the prodrugs of sulopenem to treat a disorder such as an infection in a patient in need thereof.
US7173026 Pyrrolo [2,1-c][1,4]benzodiazepine-anthraquinone conjugates useful as antitumour agents The present invention relates to synthesis of pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone hybrids (V) wherein n=3,4; R=H, OH and to their use as antitumour agents.
US20120183576 Modified gram-negative bacteria for use as vaccines The invention relates to Gram-negative bacteria carrying an inactivated gene encoding a glycosyltransferase involved in the synthesis of the core of the LPS of said Gram-negative bacteria, wherein said inactivated gene results in the synthesis of a LPS having a modified core. These strains have an attenuated virulence but induce a humoral immunity sufficient for ensuring vaccination of the host.
WO2008044767A1 Aromatic amine derivative and use thereof Disclosed is a novel SCD inhibitor. The SCD inhibitor comprises a compound represented by the formula [I], a salt thereof, or a prodrug of the compound or the salt. wherein the ring A represents an aromatic ring which may be substituted; the ring B represents a ring which may be substituted; the ring C represents an aromatic ring which may be substituted; R represents a hydrogen atom, a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; and X represents a spacer having a main chain composed of 1 to 5 atoms.
CN102755324A Pharmaceutical composition containing prasugrel and rosuvastatin, and purpose thereof The invention belongs to the field of medicines, and discloses a pharmaceutical composition used for treating cardiovascular and cerebrovascular diseases. According to the pharmaceutical composition provided by the invention, prasugrel or a pharmaceutically acceptable salt thereof, and rosuvastatin or a pharmaceutically acceptable salt thereof are adopted as pharmaceutically active ingredients. Rosuvastatin or the pharmaceutically acceptable salt thereof is calculated according to rosuvastatin, and prasugrel or the pharmaceutically acceptable salt thereof is calculated according to prasugrel. In the pharmaceutical composition, the weight ratio of rosuvastatin to prasugrel is 1:0.01-100, and preferably 1:0.2-20. When the pharmaceutical composition is applied in treating cardiovascular and cerebrovascular diseases, the effect is comprehensive, the toxic and side effects are low, and patient compliance can be improved. Therefore, the pharmaceutical composition has good medical application prospect.
EP1196050B2 Compositions for providing and maintaining energy and mental alertness The present invention relates to compositions which provide an onset and steady maintenance of energy to the consumer, as well as kits comprising the compositions and methods of using the compositions. In particular, the compositions of the present invention comprises a select mixture of carbohydrates which provides immediate and sustained energy when consumed. The compositions may optionally, but preferably, comprise one or more bracers and/or flavanols which, in combination with the foregoing select mixture, provide sustained energy and mental alertness without nervousness or tension.
WO2010046710A1 Therapeutics for neurological disorders The present invention relates to therapeutic compounds that are Nrf2-ARE pathway activators suitable for the treatment of diseases known to be mediated by oxidative stress such as motor neurone disease. The invention also includes compounds identified by the methods of the invention for treatment of neurodegenerative diseases.
US8658207 Extended release tablet formulations of flibanserin and method for manufacturing the same The present invention provides pharmaceutical release systems comprising an therapeutically effective amount of flibanserin and at least one pharmaceutically acceptable excipient, characterized in that said pharmaceutical release systems exhibit a pharmacokinetic profile that is characterized by an average maximum flibanserin plasma concentration Cmax lower than 300 ng/mL, preferably lower than 200 ng/mL after administration of a single dose to healthy volunteers in fasted state or directly after a meal.
CA2285985C A method for preparing aqueous liposomal compositions comprising an active ingredient which is highly insoluble in water Aqueous pharmaceutical composition comprising an active ingredient which is highly insoluble in water, dispersed in liposomes and method of preparation thereof.
EP1632248A1 Anti-interleukin-9 antibody or anti-interleukin-9 receptor antibody for treating bronchial hyper-responsiveness The present invention relates to the use of an antibody, which is an anti-interleukin-9 antibody or an anti-interleukin-9 receptor antibody, that blocks interleukin-9 binding to the interleukin-9 receptor, for the preparation of a medicament for the reduction of bronchial hyper-responsiveness in a patient.
US20080199540 Orally-administrable compositions comprising stable amorphous calcium carbonate The present invention provides orally-administrable compositions comprising stable amorphous calcium carbonate (ACC). The compositions are preferably prepared as solid dosage forms such as tablets, capsules and powders. The present invention further provides methods for supplementing oral calcium intake in subjects and as well as methods for treating osteoporosis, osteomalacia and related diseases.
CN1965847A Amikacin solution containing clustered water used for animal The invention relates to a method for using Amikeshen to prepare wide-spectrum antibiosis solution, wherein it uses hexacyclic ring water as carrier that adds frozen hexacyclic ring water into Amikeshen solution, to reduce the volume of hydrone group, the viscosity and surface tension, to reduce the expand resistance and accelerate the drug release. The hexacyclic ring water has strong affinity with cell, to improve the treatment effect on animal bacterial and mycoplasma affection.
US20100240727 Model for Glutamate Racemase Inhibitors and Glutamate Racemase Antibacterial Agents The increase in antibacterial resistance has created the demand for new antibiotics. The present invention relates to a more potent antibiotic that targets the enzyme glutamate racemase from known glutamate racemase inhibitors. Glutamate racemase catalyses the interconversion of L-glutamate to D-glutamate, making D-glutamate available, which is required for bacterial peptidoglycan biosynthesis. Knockout mutations have shown glutamate racemase to be necessary for bacterial cell survival and, before the present invention, no antibiotic on the market targeted this enzyme. The present invention relates to new, ligand based glutamate racemase inhibitors, developed using software to extract a pharmacophore model from a group of known glutamate racemase inhibitors. Forty-seven (47) known inhibitors were collected from the literature and several pharmacophore models were extracted therefrom. The functional groups common to all the known inhibitors were included in a pharmacophore model that described the requirements for glutamate racemase inhibition with 82% accuracy. Of these models, one was found to describe the requirements for glutamate racemase inhibition with 82% accuracy. The model was used to search databases of commercially available chemical compounds and 2-(2-(1H-indol-3-yl)ethylamino)-4-oxo-4-p-tolylbutanoic acid and 2-(2-(1H-indol-3-yl)ethylamino)-4-(4-fluorophenyl)-4-oxobutanoic acid were identified as showing antibacterial activity. These compounds were assayed against S. pneumoniae and were shown to have antibacterial activity against the non-virulent strain R6 and against a multidrug resistant strain.
US7442697 4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
WO2014070014A1 Methods and compositions for stimulating beneficial bacteria in the gastrointestinal tract The invention relates to supporting the growth or maintenance of oxygen-sensitive bacteria in the gastrointestinal tract of an animal. Provided is the use of riboflavin, riboflavin phosphate or a salt thereof, for the manufacture of a food composition, pharmaceutical composition, food or dietary supplement, for the selective stimulation of Faecalibacterium prausnitzii in the gastrointestinal tract. Also provided is a synbiotic composition comprising living beneficial butyrate- producing anaerobic bacteria formulated with riboflavin, riboflavin phosphate or a salt thereof, and cysteine.
CA2523216C Recombinant alphavirus vectors The present invention provides composition and methods for utilizing recombinant alphavirus vectors.
US20120121572 New medicines for topic use based on sulfated hyaluronic acid as activating or inhibiting agent of the cytokine activity The object of the present invention relates to the new and surprising use of sulfated hyaluronic acid (HAS) as regulator agent of the cytokine activity (pro- and anti-inflammatory) and consequently the use of HAS for the preparation of a new medicine for topic use in the prevention and treatment of pathologies associated with the activation and/or deficiency of cytokines of a pro- and anti-inflammatory nature. The Applicant has in fact discovered the exclusive capacity of HAS in modulating the activity of these particular proteins, it has studied the action mechanism and demonstrated the substantial difference between the different sulfated types known in the state of the art, but above all it has demonstrated an unexpectedly high activity of HAS vs different types and strains of Herpes virus, Cytomegalovirus and the virus of vesicular stomatitis. Finally, a further object of the present invention is the use of HAS as a skin absorption promoter of drugs of an anti-inflammatory nature.
US20110065687 Hydrazide compounds and uses thereof This application relates to certain novel polycyclic compounds that interact with quadruplex-forming regions of polynucleotides and thereby inhibit translation of genetic information into polypeptides. These compounds can thus provide anticancer and antibacterial and antiviral effects. The invention includes novel compounds and pharmaceutical compositions, and methods of using them to treat cancer and other conditions.
CN1579376A Rhizoma-curcumae-longae element-soft cap sule and its preparation method The invention discloses a safe and high efficient blood-fat regulating medicine and its manufacturing method. The invented curcumin soft capsule is filled with curcumin and plant oil or polyethylene glycol, the weight proportion is 1:3-6; the shell of the soft capsule is made up of alum, glycerin, and water, the weight proportion is 40-60:10-30:50-30The manufacturing method is: the curcumin is crashed into powder, and extracts with supercritical CO2, the deoiled curcumin A is put into alcohol or acetone and acquires the curcumin B; takes the curcumin extracts accordant to content demands, adds in 3-6 times of plant oil or polyethylene glycol, produces the content of the soft capsule; takes the alum, glycerin, and water according to the proportion; blends them and produces the capsule shell of the soft capsule; compresses the soft capsule. The effective content of the is high, it has more excellent effect.
US6869969 Isoxazole estrogen receptor agonist and antagonist Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
CN101759741A Compound and application thereof in preparation of medicine for treating angiogenesis The invention relates to a compound and application thereof in preparation of medicine for treating angiogenesis, and the compound is shown in formula (1), wherein R2 is a hydrocarbon group which contains 1-2 heteroatom(s) and has less than or equal to ten carbon atoms. The compound is prepared by carrying out acylation reaction 21 on compound in formula (1.1). The compound shown in the formula (1) and solvate thereof which can be acceptable in physiology can be used for preparing medicine for treating age-related macular degeneration and the medicine for treating diseases caused by angiogenesis of human being or animals.
CA2594251A1 Pyrrolidyl derivatives of heteroaromatic compounds as phosphodiesterase inhibitors The invention pertains to new pyrrolidyl derivatives of benzo-fused aza heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds that are selective inhibitors of PDE-IO. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom. Formula (I).
US20110014271 Substituted Aniline Derivatives The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
CN103239436A Application of isorhamnetin to preparing drugs for adriamycin adjuvant therapy The invention discloses new drug application of adriamycin and particularly discloses the application of adriamycin to preparing drugs for the adjuvant therapy of tumor patients taking adriamycin for a long term in clinic.
CN102015700A Antibacterial condensed thiazoles Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (-O-), thioether (-S-) or amino (-NR)- link, wherein R is hydrogen, -CN or C1-C3 alky!; X is -C(=O)NR6-, or -C(=O)O- wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is -N= or -CH= Z2 is -N= or -C(R1)=; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkOXy or (C1-C2)alkylthio, nitro, or nitrile (-CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (-O-), thioether (-S-) or amino (-NR)- link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 5 or 6 ring atoms or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 9 or 10 ring atoms; Q1 is hydrogen, an optional substituent, or an optionally substituted carbocyclic or heterocyclic radical having 3-7 ring atoms.
CN103333156A Preparation method of 2-substituted arylethenyl-N-methylated quinoline derivative and application of 2-substituted arylethenyl-N-methylated quinoline derivative in preparation of drug for treating Alzheimer disease The invention relates to the field of medicinal chemistry and pharmacotherapeutics and provides a 2-substituted arylethenyl-N-methylated quinoline derivative, a synthesis method thereof and an application of the 2-substituted arylethenyl-N-methylated quinoline derivative to the preparation of a drug for treating Alzheimer disease. The 2-substituted arylethenyl-N-methylated quinoline derivative has the chemical formula shown in the specification, wherein R1 in the formula is hydrogen, methylpiperazine, piperidine, morpholine, ethoxylpiperazine, dimethylaminoethylpiperazine or dimethylaminopropylpiperazine; R2 is para-substituted chlorine, fluorine, hydroxyl, methoxyl, dimethylamino, diethylin, methylpiperazine and morpholine, or ortho-substituted hydroxyl and methoxyl or meta-substituted methoxyl and nitro; R4 is hydrogen, chlorine, fluorine, hydroxyl, methoxyl, dimethylamino, diethylin, methylpiperazine or morpholine; R2 and R6 are hydrogen, hydroxyl or methoxyl; R3 and R5 are hydrogen, methoxyl or nitro. Experiments prove that the 2-substituted arylethenyl-N-methylated quinoline derivative provided by the invention has anticholinesterase activity, anti-Abeta aggregation and antioxidant activity.
EP1542966A1 Aromatic liver x-receptor modulators The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula (I) and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula (I).
US20100152136 TP53 Gene expression and uses thereof The present invention is drawn to diagnosis, prognosis and treatment of multiple myeloma. In this regard, the present invention discloses importance of down-regulation of TP3 gene in multiple myeloma and its use as an independent progostic indicator of multiple myeloma. Additionally, the present invention also discloses novel-TP53 associated genes and demonstrates the clinical relevance of these alterations to disease progression.
US20090104272 Inhaled hypertonic saline delivered by a heated nasal cannula The invention described herein is directed to method of treating chronic obstructive pulmonary disease, comprising administering an effective amount of an osmolyte by at least one nasal cannula to a subject in need thereof. Also provided is a nasal cannula system for delivering an osmolyte, comprising a nebulizer and tubing having two ends, where the first end of the tubing is connected to the nebulizer and the second end of the tubing is tapered to fit in the nostril of a subject.
WO2014002553A1 Aripiprazole oral pharmaceutical preparation The purpose of the present invention is to provide an aripiprazole oral pharmaceutical preparation which has limited acidity and bitterness, poses little burden to the patient when administered, and is highly elutable, and for which the patient himself can readily confirm administration. The present invention pertains to an oral pharmaceutical preparation characterized by containing aripiprazole and a gelling agent, the pH being 4.6 or higher.
WO2013023563A1 Use of potassium piperonyl pentadienoate for lowering blood lipid The invention provides the use of potassium piperonyl pentadienoate for lowering blood lipid, including the use of the potassium piperonyl pentadienoate in the preparation of medicaments and health-care products for lowering serum total cholesterol, lowering low density lipoprotein cholesterol, lowering triglyceride as well as preventing the decrease of high density lipoprotein cholesterol.
CN103301130A Method for inducing dog to rut in anestrous season The invention discloses a method for inducing a dog to rut in an anestrous season. The method is characterized by comprising the following steps of: continuously feeding bromocriptine in a vagina for 20 days according to the amount of 0.6mg per dog and feeding one time per day; in the seventh day of rutting, injecting hCG500IU per dog into muscle for one time; and naturally mating, wherein the pregnancy rate reaches 87.50% and the farrowing rate reaches 96.43%. The E2 and P4 concentrations in estrus induction dog blood serum are equal to those of natural rutting. The effect of adding the bromocriptine into the vagina is better than that of oral taking, so that the bad gastrointestinal reaction can be overcome and the estrus induction rate can be increased. The method disclosed by the invention proves that bromocriptine vagina feeding is a simple, feasible and effective method for inducing the dog to rut in the anestrous season.
EP2318012A2 Methods and compositions for treating and preventing autoimmune diseases Provided are methods and compositions for treating and/or preventing an autoimmune diseases, including inflammatory bowel disease, rheumatoid arthritis, diabetes mellitus, celiac disease, autoimmune thyroid disease, autoimmune liver disease, Addison's Disease, Sjögren's Syndrome, transplant rejection, graft vs. host disease, or host vs. graft disease.
US20110172302 Methods of treating meibomian gland dysfunction The present invention includes methods for treating Meibomian gland dysfunctions. The invention also includes methods for improving tear lipid composition, for treating abnormal Meibomian gland secretion and for normalizing Meibomian gland secretions.
US20110319805 Topical composition for treating the skin The present invention relates to a topical composition for the treatment of mammals suffering from a condition of the skin such as a skin lesion, a wound, a cut, an abrasion, a hot spot, a sore foot pad, inflamed skin or dry skin; wherein the composition contains a blend of four separate creams, a steroidal material, a normally injectable vitamin A and vitamin D composition, an antibiotic material and, optionally, ingredients such as aloe vera, an antifungal agent, an anti-parasitic agent, DMSO and a topical anaesthetic.
US7713941 Tricyclic nucleosides or nucleotides as therapeutic agents Nucelosides and nucleotides containing a tricyclic base portion thereof are useful for treating infectious diseases and proliferative disorders, such as viral infections or cancer respectively.
WO2011034832A1 Substituted phenoxymethyl dihydro oxazolopyrimidinones, preparation and use thereof The present invention relates to a series of substituted phenoxymethyl dihydro oxazolopyrimidinones of formula (I) defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
CN102232931A Formula of asarone for injection and preparation method thereof The invention provides a formula of asarone for injection and a preparation method thereof. In the invention, an injection is prepared by using asarone as a main ingredient, Tween-80 and polyethylene glycol (PEG)-400 as solubilizer and mannitol as an excipient, and the solubility of the asarone is improved effectively; and thus, the medicine carrying capacity of the injection is increased. The injection prepared by the invention has high re-solubility and product stability, and the preparation process is simple.
CN102973560A Novel method of applying matrine to treating eczematous dermatitis The invention provides a novel method of applying matrine to treating eczematous dermatitis, belonging to the field of medicines. The method is characterized by 1. adopting intravenous drip of matrine to treat eczematous dermatitis, 2. adopting intravenous drip of matrine to treat eczematous dermatitis in combination with oral administration of antihistamines, 3. adopting oral administration of matrine tablets or capsules to treat eczematous dermatitis and 4. applying matrine ointments to the wounded parts to externally treat eczematous dermatitis. Compared with the existing medicines and methods for treating eczematous dermatitis, the novel method has the effects that unexpected curative effects can be obtained and the cure rate is above 75%. The new method is an innovative idea of holistic treatment for treating eczematous dermatitis and has great medical significance.
EP1957468A2 Polyalkylene glycol derivatives of 4 - (phenylamino)quinazolines useful as irreversible inhibitors of epidermal growth factor receptor tyrosine kinase Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK irreversible inhibitors as their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are further disclosed. The disclosed EGFR-TK irreversible inhibitors comprise a polyalkylene glycol moiety and are characterized by improved solubility, biostability and bioavailability.
EP1462442B1 Crystals of bicalutamide and process for their production The invention relates to crystals of bicalutamide having a specific crystal form, and industrially practicable processes for the production of bicalutamide and crystals thereof which are excellent in environmental friendliness, economical efficiency, and safeness. The invention provides a process for the production of bicalutamide represented by formula (1): (1) characterized by comprising at least the step of reacting a compound represented by formula (3) with an oxidizing agent: (3) a process for the production of crystals of bicalutamide; and a crystal form of bicalutamide as determined by X-ray diffraction (XRD) or solid-state 13C NMR spectroscopy.
EP1592427A1 Multivitamin regimen for renal patients A vitamin and mineral supplement regimen for dialysis patients. The regimen comprises first and second formulations. The first formulation contains selenium, and no zinc, and is administered on days of dialysis. The second formulation contains zinc, and no selenium, and is administered on days between dialysis. In addition, the second formulation contains more vitamin C and folic acid than the first formulation.
US20080032944 Target Nucleic Acid Of Retrovirus Integration A nucleic acid that is a target of retrovirus integration and has a substantially palindromic sequence that includes a motif sequence: 5′-α1-α2- . . . -αn-X-βn- . . . -β2-β1-3′, wherein α1 to αn each represent a sequence consisting of contiguous 4 to 7 bases in 5′-CACAGTG-3′ or 5′-CACTGTG-3′, X represents an arbitrary sequence consisting of 0 to 10 bases, β1 to βn each represent a sequence consisting of 4 to 7 bases substantially complementary, in the opposite direction, to the sequence α1 to αn, respectively, n represents an integer of 1 or more, and an arbitrary sequence consisting of one to a few bases may be present between the adjacent sequences among the sequences α1 to αn and β1 to βn; and upstream and downstream sequences adjacent to the motif sequence, having a length of 2 bases or more.
US20100331337 Quercetin-Containing Compositions This invention relates to a composition containing quercetin, vitamin B3, vitamin C, and folic acid. Also disclosed is a method of using the composition for enhancing physical or mental performance or treating various diseases or disorders.
CN101574326A Capsule preparation containing tegafur, Jimeisita and Potassium Oxonate and preparation method thereof The invention relates to a capsule preparation containing tegafur, Jimeisita and Potassium Oxonate and a preparation method thereof, which is characterized in that the capsule preparation contains tegafu micropill, Jimeisita micropill and Potassium Oxonate micropill, wherein, the micropill is prepared from active drug ingredient, thinner, bond and surface active agent. The micropill is prepared with the extruding-rolling method, the centrifugal-fluidifying method, the pan coating pill floating method and the like, and then, other minor ingredients are added; finally, the capsule is filled. The capsule prepared with the preparation method can be steadily and quickly released in bodies, thus the drug stability is improved. The capsule has high dissolution rate and biological availability, and reduces adverse reaction of medicine.
US20100035870 Pyrimidin-4-yl-3, 4-Dihydro-2H-Pyrrolo[1,2A] Pyrazin-1-one Compounds The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, wherein Z is NR11, NHCO, NHSO2, NHCH2, CH2, CH2CH2, or CH═CH; X is a hydrocarbyl group optionally substituted by one or more R12 groups; R10 and R11 are each independently II or alkyl; R1-R4 are each independently II or (CII2)mR12, where m is O, 1, 2, or 3; each R12 is independently (CH2)aR16, where each R16 is independently selected from O(CH2)bR13, R13, COR13, COOR13, CN, CONR13R14, NR13R14, NR13COR14, SR13, SOR13, SO2R13, NR13SO2R14, SO2OR13, SO2NR13R14, halogen, CF3, and NO2, and wherein each a is 0, 1, 2, or 3 and b is 0, 1, 2, or 3; R13 and R14 are each independently H or (CH2)nR15, where n is 0, 1, 2, or 3; and each R15 is independently selected from alkyl, cycloalkyl, heteroaryl, aralkyl, aryl and heterocycloalkyl, each of which may be optionally substituted by one or more substituents selected from halogen, OH, CN, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO— alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy, wherein said alkyl and alkoxy groups may be further substituted by one or more OH groups. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula I, and the use of compounds of formula (I) in the preparation of a medicament for treating a variety of disorders, including proliferative disorders, viral disorders, stroke, etc.
CN1813941A Chinese and western compounded drug for treating alveolysis and its preparing method The present invention discloses a medicine composition for effectively curing odontopathy and its preparation process. It is made up by using metronidazole, erythromycin, prednisone, crude gypsum, cimicifuga root and asarum as raw material through a certain preparation process. It can be made into capsule preparation, and its effective rate is above 95%.
CA2239519C Specific binding members for human carcinoembryonic antigen, materials and methods Sequence and binding information is provided for particularly advantageous specific binding members which bind human carcinoembryonic antigen (CEA) with a dissociation constant which is less than 1,0 × 10 -8M, are substantially non-cross-reactive with human liver cells, bind to the A3-B3 extracellular domain of human carcinoembryonic antigen and/or bind to cell-associated human carcinoembryonic antigen preferentially over soluble human carcinoembryonic antigen. These are useful particularly in determination of CEA expression by cells such as tumour cells.
US20070232538 Uses of polypeptides The present invention provides uses of a polypeptide having a ligand activity to a sensory epithelium neuropeptide-like receptor (SENR) which is a G protein-coupled receptor protein, and a DNA encoding the same. More specifically, the present invention provides an anti-attention-deficit-disorder or anti-narcolepsy agent, which comprises a polypeptide having a ligand activity for SENR or a salt thereof, as well as a method for screening compounds having an anti-attention-deficit-disorder or anti-narcolepsy activity or compounds having an anti-anxiety, anti-depression, anti-insomnia, anti-schizophrenia or anti-fear activity or salts thereof, which comprises using the above polypeptide or a precursor protein of the polypeptide or a salt thereof.
CN102657659A Transdermally-absorbed medicament used for skin and consisting of adjuvant-containing fluticasone propionate and adjuvant-containing water A transdermally-absorbed medicament used for skin and consisting of adjuvant-containing fluticasone propionate and adjuvant-containing water comprises: fluticasone propionate which is single packaged and water-insoluable, has a D90 particle size of 0.1 to 10 [mu]m, and contains one or a plurality of solid pharmaceutic adjuvants; and water which is single packaged and contains one or a plurality of water-soluable pharmaceutic adjuvants.
CN101497653A Small peptide for inhibiting solid tumor and leukaemia cancer cell growth and use thereof The invention provides a short peptide for inhibiting the solid tumor and the growth of the cancer cells of leukemia. The amino acid main sequence of the short peptide fragment, the analogue, the derivative and the variant of the short peptide has the sameness being equal to or more than 70 percent of the amino acid main sequence of the short peptide and has the similarity being equal to or more than 90 percent of the amino acid main sequence of the short peptide; and the short peptide, the nucleotide, the short peptide fragment, the short peptide analogue, the short peptide derivative and the short peptide variant are used for preparing drugs for curing the leukemia caused by hyperplasia of various pthological cells of the non-solid tumor human myeloblast, curing various cancers of cancer cell multiplication of the human solid tumor and diagnosing and detecting the occurrence of the cancer as well as the grade malignancy of occurrence of the cancer, and the short peptide or the nucleotide is used for preparing the drugs as the protease inhibitor, the promoter or the nucleophilic reagent or detecting the detection of the application of the reagent. The technology can solve the problem that the prior cancer drug has serious harm to the normal cells of the human body when inhibiting or killing the cancer cells.
EP2035007A1 Use of adenosine a1 antagonist in radiocontrast media induced nephropathy The present invention relates to pharmaceutical combinations comprising a therapeutically effective amount of at least one selective adenosine A1 antagonist and at least one radiocontrast media. In particular, the present invention relates to pharmaceutical combinations comprising 4-[(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-trans-cyclohexanol methanesulfonate and/or (4S)-4-hydroxy-1-(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-L- prolinamide methanesulfonate as selective adenosine A1 antagonists and at least one radiocontrast media. The invention also relates to the use of said combinations in the manufacture of a medicament for the treatment of radiocontrast media induced nephropathy. Furthermore, the invention is relating to a kit comprising a therapeutically effective amount of said combination of at least one selective adenosine A1 antagonist and at least one radiocontrast media.
US7479503 Such as multiple sclerosis; also inactivating HIV virus via extracorporeal treatment of blood; use of a green porphyrin or porfimer sodium Multiple sclerosis and rheumatoid arthritis can be treated effectively using photodynamic therapy. In this protocol, a photoactive compound is administered, allowed to distribute in the effected subject, and the subject is then irradiated to activate the photoactive compound. Alternatively, the blood of a subject to be treated can be subjected to PDT extracorporeally. In the case of rheumatoid arthritis, localized treatment at the joints may also be employed.
WO2008041003A3 Hydroxycholesterols and its prodrugs for the treatment of insulin resistance and disorers asociated therewith The present invention provides the use of an LXR antagonist, or a physiologically- acceptable pro-drug therefor, in the manufacture of a medicament for combating insulin resistance or a disorder associated therewith. Further provided is a compound being an ester or carbamate of a hydroxycholesterol, a pharmaceutical composition of such a compound or its use in therapy.
CN1935821A Antibacterial compound and its use The invention discloses the compound showed as formula I and its pharmacy acceptable salt form, use of antibiosis.
US7144917 For therapy and prophylaxis of cancer, angiogenesis, arthritis, connective tissue disease, cardiovascular disease, inflammation or autoimmune disease in a mammal The invention provides compounds that inhibit MMPs; methods for treating or preventing cancer, angiogenesis, arthritis, connective tissue disease, cardiovascular disease, inflammation or autoimmune disease in a mammal; a method for inhibiting a matrix metalloproteinase in vivo or in vitro; and a method for imaging a tumor in vivo or in vitro.
CN101537038A Pharmaceutical composition for preventing and curing children cold and preparation method thereof The invention discloses a pharmaceutical composition for preventing and curing children cold and a preparation method thereof. The pharmaceutical composition is prepared by the following bulk drugs according to proportioning by weight: 10-100g of liquorice, 30-100g of balloonflower root, 10-100 mg of artificial cow-bezoar and 2-20mg of chlorphenamine maleate. The invention has the effects of clearing away heat and toxic material and eliminating phlegm and stopping cough, is used for curing various symptoms such as fever, cough, headache, stuffy nose, watery nasal discharge, sneezing, throat difficulties, and the like caused by the children cold and flu, and has definite therapeutic effect.
EP1505971A2 Administration of acetylcholinesterase inhibitors to the cerebral spinal fluid Methods and compositions are disclosed that provide acetylcholinesterase inhibitors for the prevention and treatment of diseases and disorders of the central nervous system, including dementia such as Alzheimer's disease, to the central nervous system via intranasal delivery. The methods and compositions of the present invention provide therapeutic concentrations of the acetylcholinesterase inhibitor in the cerebrospinal fluid of a mammal without the attendant disadvantages, risks and side effects of oral or injection delivery.
CN101019956A Bedsore treating medicine The present invention discloses one kind of bedsore treating medicine. The medicine is prepared with Chinese goldthread 80-120 weight portions, skullcap root 80-120 weight portions, phellodendron bark 80-120 weight portions, and borneol 3-6 weight portions, and through grinding into fine powder, 20 mesh sieving and sealing preservation. The medicine has the functions of clearing away heat and toxic material, astringing, promoting granulation, etc, so that it has excellent curative effect on bedsore.
WO2013135571A1 Compositions with enhanced therapeutic efficacy against infective agents of the eye comprising miltefosine and polyhexamethylene biguanide An antibiotic composition comprising miltefosine and polyhexamethylene biguanide (PHMB) and its use in the prevention or treatment of a condition of the eye or the skin is provided by the present invention.
WO2012097054A1 Methods and compositions for treating cancer and related methods The present invention relates to anti-cancer therapeutics. In certain aspects, cancers are treated with a combination of an anti-EGFR agent and an agent that increases the activity of the KLF6 tumor suppressor gene and/or an agent that increases activity of the FOXO1 tumor suppressor gene. In a preferred aspect, the anti-EGFR agent erlotinib a tricyclic agent compound, are used in combination to treat non-small cell lung cancer in a patient with primary or acquired drug resistance to erlotinib, and wherein the tricyclic agent is administered in an amount that does not lead to a substantial central nervous system effect. In additional aspects, the invention relates to compositions and kits useful for treating cancers, methods for screening for compounds that enhance the activity of anti-EGFR agent, and methods for determining whether a patient will respond to anti-EGFR therapy.
US20120316121 Materials and Methods for Modulating Arginine Metabolism The present invention provides novel compositions and methods for their production and use in modulating arginine metabolism to treat biological conditions. The biological condition is preferably one associated with dysregulated arginine metabolism and/or abnormal endogenous levels of substances resulting from or involved in arginine metabolism. The subject invention provides compositions that modulate levels of arginine or levels of substances that are derived from arginine in vivo via pre-selected signal transduction/metabolic pathways. In one embodiment, compositions comprising arginine and a glycoside are provided. The compositions and methods of the invention are able to select and prompt a particular metabolic pathway in which the arginine is to be used as a substrate.
US20130012479 Polymorphs of 6-(piperidin-4-yloxy)-2h-isoquinolin-1-one hydrochloride The present invention relates to new crystalline polymorphs of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and their use, in particular for the preparation of medicaments.
EP1737880A1 17alpha-fluoro-17beta-hydroximinomethyl steroids, a method for production thereof and pharmaceutical compositions comprising said compounds The invention relates to 17α-fluorosteroids of general formula (I), where R1 = H or CH3, R2 and R3 = H, Cl or CH3 and a single- or double-bond is arranged between carbon atoms 6 and 7 and between 9 and 10 and pharmaceutical compositions comprising said compounds. Said compounds have an activity profile with a hybrid character, acting as 5α-reductase inhibitors and simultaneously as high-potency gestagens and are thus suitable for the treatment of diseases in certain organs and tissues of men and women resulting form a high concentration of androgens. In connection with other hormonal substances, such as oestrogen, testosterone or another strong androgen, said compounds are suitable for use as contraceptives and other similar applications in men and women.
US20110104226 Peptides having binding affinity to an antibody which recognizes an epitope on an a1 loop 2 or beta2 loop 1 of an adrenoreceptor A peptide having an ED50 of less than 500 nm, in particular 10 nM to an antibody which recognizes an epitope on an extracellular α1 loop 2 or β2 loop 1 of a human adrenoceptor wherein the antibody's binding to the epitope results in an increase of γ-secretase activity, an increased release of β-amyolid molecules and/or cellular dysfunction of cerebral blood vessel cells, glia cells or neurons, wherein the ED50 value is measured by bioassay.
WO2008044656A1 Imidazolidinone derivative Disclosed is an imidazolidinone derivative represented by the formula (1), a pharmaceutically acceptable salt thereof, or a hydrate of the derivative or the salt, which has a satisfactory therapeutic effect that relies on a 11β-HSD1-inhibiting activity. (1) wherein A represents an aromatic hydrocarbon ring; R1 and R2 and R3 independently represent a hydrogen atom, a halogen atom, a trifluoromethyl group, a C1-4 alkyl group, a trifluoromethoxy group, or a C1-4 alkoxy group; R4 represents a C1-4 alkyl group; and X represents a hydroxyl group, a C2-5 alkoxycarbonyl group, acarboxyl group, or a carbamoyl group.
US20080045561 protein kinase inhibitors such as 5,6-Dimethoxy-1-methyl-3-(1H-pyrrolo[2,3-b]pyridin-2-yl)-1H-pyrrolo[3,2-b]pyridine, used for the treatment of cancer Disclosed are compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.
CN103347509A Compound and composition for treatment of cancer New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of a combination of two of these compounds is described and the use of the combination of one of these compounds with an anticancer agent such as decarbazine, doxorubicin, daunorubicin, cyclophosphamide, busulfex, busulfan, vinblastine, vincristine, bleomycin, etoposide, topotecan, irinotecan, taxotere, taxol, 5-fluorouracil, methotrexate, gemcitabine, cisplatin, carboplatin and chlorambucil.
WO2006042890A1 Therapeutic composition for the treatment of burns The invention relates to a therapeutic composition for the treatment of burns. The inventive composition comprises liquid lead subacetate, aluminium potassium sulphate, vinegar, a colony, anise and water in the following weight percentages: between 0.2 and 1 % liquid lead subacetate, between 0.1 and 0.5 % aluminium potassium sulphate, between 8 and 12 % of a colony, between 3 and 7 % anise, and between 17 and 23 % vinegar, the remainder being water.
US20110086903 Emergence of a r-type ca2+ channel (cav 2.3) contributes to cerebral artery constriction following subarachnoid hemorrhage The invention relates to methods and products for treatment of a neurological defect such as a subarachnoid hemorrhage or cerebral vasospasm. Specifically, R-type voltage-gated calcium channel inhibitors and related compositions and kits are described.
WO2010120880A1 Treatment of liver diseases with a caspase inhibitor The present disclosure provides a method of using VX-166, a pan caspase inhibitor, for treating or reducing the symptoms of liver diseases, such as Non- Alcoholic Fatty Liver Disease (NAFLD), nonalcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), and other diseases involving fibrosis, steatosis, or inflammation of the liver. The present disclosure also relates to methods for identifying agents useful for treating these diseases. The present disclosure also relates to additional therapeutics that can be used in combination with VX-166 for the treatment of these diseases.
WO2006035900A1 Coenzyme q10-containing emulsified composition Disclosed is an emulsified composition containing coenzyme Q10 which is excellent in storage stability and solubility or dispersibility in water. Also disclosed is an emulsified composition containing coenzyme Q10 which is well absorbed in the body. Such an emulsified composition can be prepared by emulsifying coenzyme Q10 into a certain amount of water using a certain amount of a medium-chain triglyceride, a surfactant and a polyhydric alcohol.
US7049336 Method for diagnosing neuronal diseases and for treating primary hemostasis deficiency Pharmaceutical compositions for treatment of primary hemostasis deficiency and methods of treatment of primary hemostasis deficiency are disclosed. Also, methods for diagnosing neuronal diseases and for suppressing the immune system are disclosed. Isoforms responsible for maintaining primary hemostasis, T-cell mediated immune responses, neuron specific TPH, and a neuronal tryptophan hydroxylase are disclosed.
US20060167026 Antipsychotic molecular-targeting epithelial growth factor receptor The purpose of this invention is to provide an agent useful for prevention and/or treatment of psychosis, schizophrenia and cognitive impairments. To solve this problem, this invention provides epidermal growth factor receptor inhibitors as therapeutic agents for psychosis, schizophrenia and cognitive impairments.
CN101683498A Preparation method of pill for dispelling yellowish complexion and eliminating swelling The invention relates to a preparation method of a pill for dispelling yellowish complexion and eliminating swelling. The pill has the functions of warming the spleen and stomach, purging dampness andheat and regulating qi and eliminating dampness, and has good using effect on patients with persistent hepatitis and hepatosplenomegaly.
CN101104609A Solanesyl polyamine derivative, preparation and application thereof The invention discloses solanesyl polyamines derivatives which are compounds with the following common structural formula, wherein, n is equal to 0-2, Ar is phenyl, substitutive phenyl, 1-naphthyl, 2-naphthyl, 9-anthryl or tricyclic aryl containing N,S atoms. The preparation method is as follows: dissolve N-solanesyl-N amine alkyl piperazine in organic solvent; add aromatic aldehyde and make the mixture react for 2-24 hours under the temperature of 0-20 DEG C; steam the mixture to get rid of the solvent and then add reducer when bathing the mixture in ice water and let the mixture react for 2-12 hours under room temperature; process the products and separate the products by column chromatography to get the solanesyl polyamines derivative. The invention provides a series of new solanesyl polyamines derivatives which are the homologous derivatives of natural products, maintain the original all-trans stereo configuration of the solanesol unit and can be used as anti-neoplastic drugs and primer for the anti-neoplastic drugs. The preparation method of the invention is of simple operation with moderate condition and high reaction yield and with great market potential, thus is easy to be industrialized.
WO2014039899A1 Pyrazolopyrimidine compounds as kinase inhibitors The present disclosure provides compounds of Formula (IA) and/ or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
US7727527 Anti-NGF antibodies for the therapeutic treatments The present invention relates generally to methods of using anti-NGF antibodies in the treatment of various NGF-related disorders, including asthma, arthritis and psoriasis. The methods are effective in treating these disorders in a patient without having a significant adverse effect on the immune system of the patient.
WO2011083998A2 Biguanide derivative, a preparation method thereof and a pharmaceutical composition containing the biguanide derivative as an active ingredient The present invention provides a biguanide derivative or pharmaceutically allowable salt thereof represented by Formula 1 with N1-N5 substitution, a preparation method thereof and a pharmaceutical composition containing the biguanide derivative as an active ingredient. Compared with conventional drugs, even a small amount of the biguanide derivative of the present invention exhibits excellent effects of AMPKα activation and inhibition of cancer cell proliferation, which makes it useful for the treatment of diabetes, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer and the like.
CN101023977A Slow-released tablet floating in stomach for treating gastric disease The present invention discloses an endogastric flotation slow release tablet for curing gastritis. Said slow release tablet is obtained by using 20 g of licorice flavone, 20-30 g of hydrophilic gel skeleton material, 5 g of pore-forming agent and 10-20 g of flotation adjuvant, and using 80% ethyl alcohol as adhesive to make the above-mentioned materials into a soft material, sieving the above-mentioned soft material by using sieve with 18 meshes, making granules, drying at 40 deg.C, finishing granules by using sieve with 18 meshes, adding proper quantity of magnesium stearate, uniformly mixing them, tabletting so as to obtain the invented product. The described hydrophilic gel skeleton material is hydroxypropyl methyl cellulose (HPMC) and carboxymethyl cellulose sodium (CMC-Na), the pore-forming agent is PEG-6000, and the flotation adjuvant is octadecanol or hexadecanol.
CN101768150A 2-[3-cyano-4-isobutoxy phenyl]-4-methylthiazol-5-formic acid crystal forms and preparation method thereof The invention discloses three crystal forms of a hyperuricemia resistant medicament 2-[3-cyano-4-isobutoxy phenyl]-4-methylthiazol-5-formic acid and a preparation method thereof. The preparation method of the crystal forms adopts frequently-used solvents such as a normal hexane-ethyl acetate mixed solvent, dichloromethane, glacial acetic acid, and the like, and the prepared crystal forms have no residual solvents and higher safety.
CN102579964A Preparation method of medicinal plaster ointment for treating jaundice The invention relates to a preparation method of a medicinal plaster ointment for treating the jaundice. The preparation method comprises the following steps: cogrinding cattail pollen, Rhizoma curcumae longae, safflower, Gardenia jasminoides ellis, talcum and the like into extremely fine powder, removing internal organs from green back crucian, baking the green back crucian and pork liver until dryness, grinding the dried green back crucian and the dried pork liver into extremely fine powder, uniformly mixing the powders, and mixing the mixed powder by rice vinegar and a liquor to prepare a paste for the externally application to the liver area. The ointment has the advantages of short treatment course, fast effectiveness, substantial effect, and no pains and side effects when the ointment is externally applied to treat the jaundice.
CN101879148A Method for preparing bacterial cellulose hydrogel temperature-reducing plaster and product thereof The invention discloses a method for preparing a bacterial cellulose hydrogel temperature-reducing plaster and a product thereof, in particular a method for preparing the repeatedly used bacterial cellulose hydrogel temperature-reducing plaster and the product thereof. The method comprises the following steps of: soaking a treated bacterial cellulose hydrogel film which reaches the medicinal level in aqueous solution of gelatin at a certain concentration, and standing for 5 to 30 minutes; and taking a part of the treated bacterial cellulose for dehydrating, packaging and sterilizing so as to obtain the bacterial cellulose hydrogel temperature-reducing plaster which is compounded by the gelatin and the bacterial cellulose. The preparation method has the characteristics of simple and practicable process, convenient operation, controllable preparation technology, no pollution, and low cost. The obtained bacterial cellulose hydrogel temperature-reducing plaster has the advantages of high biocompatibility with the skin, high moisture content, high water-retaining property, strong roughness, good air permeability, effects of cold compress physical therapy, physical temperature reduction, pain relief and the like, and convenient and safe use.
CN101724053A Human epididymis expression sperm binding protein HEL-78, encoding gene and application thereof The invention belongs to the field of biotechnology and medicine, and discloses a new human epididymis specific expression sperm binding protein HEL-78 as well as preparation and application thereof. The invention discloses an amino acid sequence of the HEL-78 protein and provides a recombination expression carrier carrying the DNA sequence for encoding the protein. The protein is located in the middle top and tail parts of a mature sperm. A RT-PCR result shows that the gene is mainly and specifically expressed in the epididymis. A band of about 72 KD is detected in the corpus epididymidis part with Western blot. The HEL-78 protein can be used as a target protein for researching and developing immunity contraceptive as well as clinical diagnosis and treatment for male sterility. A method for detecting a corresponding gene or protein based on development of the HEL-78 protein can be widely used for the research field of reproductive medicine.
US20080242667 e.g. N-(4-{4-[2-({3-[2-(4-Morpholinyl)ethyl]phenyl}amino)-4-pyrimidinyl]-1H-pyrazol-3-yl}phenyl)benzamide; serine/threonine kinase inhibitor; anticarcinogenic, antitumor agent The present invention provides a compound represented by Formula (I): or a salt thereof, or a solvate thereof, or a combination thereof, wherein the substituents are as defined herein. The present invention also relates to a composition comprising the compound of formula (I) and diluents, carriers, or excipients. Furthermore, the present invention relates to a method of treating a disease of cell proliferation comprising administering to a patient in need thereof a pharmaceutically effective amount of the compound of formula (I) or a salt thereof, or a solvate thereof, or a combination thereof.
CN103070983A Composition based on main components of Pu'er tea and application thereof The invention discloses composition based on main components of Pu'er tea and the application thereof. The composition comprises tea brown pigment, tea polysaccharide, tea polyphenol, caffeine, gamma-aminobutyric acid and gallic acid. A wild type mouse embryo fibroblast is utilized to test the killing effect of DNA toxicity chemical substance to normal cells and the effect that the composition provided by the invention protects the normal cells from DNA damage and prevents apoptosis; the result shows that the composition provided by the invention can effectively prevent the normal cell death caused by DNA toxicity chemical substance; and further research shows that the composition provided by the invention does not protect tumor cell death caused by the DNA toxicity chemical compound, conversely, the composition provided by the invention can promote the killing effect of the DNA toxicity chemical compound to the tumor cells. Therefore, the composition can be used for protecting the normal cells during the chemotherapy of tumor patients and alleviating toxic side effects caused by tumor chemotherapy, and meanwhile sensibilizes chemotherapy drug, enhances chemotherapy effect, and improves survival quality of chemotherapy patients.
CN103275128A Hydroxy phosphamide compounds of (+)-Brefeldin A, and preparation method and application thereof The invention discloses a hydroxy phosphamide compounds of (+)-Brefeldin A, and a preparation method and an application thereof. The phosphamide compounds of (+)-Brefeldin A has substantial inhibition effect on propagation of a human lung cancer A549 cell, and shows obvious concentration dependence.
WO2008087365A2 Substituted 1, 3-diphenylpropane derivatives, preparations and uses of same The invention relates to substituted 1,3-diphenylpropane derivative compounds, to pharmaceutical compositions containing same, and to the therapeutic applications thereof, especially in the fields of human and animal health.
WO2009156041A3 Thiazolyl piperdine derivatives The invention relates to compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R9, R10, R11, Q and W are as defined in claim 1 and precursors thereof are inhibitors of spingosine kinase and can be used, for instance, for the treatment of tumors.
US20110158983 Compositions and methods for mucositis and oncology therapies In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.
CN103110693A Composition capable of being used for prevention, treatment or auxiliary treatment of cardiovascular and cerebrovascular diseases or chronic diseases as well as preparation method and application thereof The invention discloses a composition capable of being used for prevention, treatment or auxiliary treatment of cardiovascular and cerebrovascular diseases or chronic diseases. The composition comprises the following components in parts by mass: 45 to 55 parts of a salvia miltiorrhiza alcohol extract, 45 to 55 parts of an eucommia bark aqueous extract, 25 to 35 parts of vitamin PP, 25 to 35 parts of vitamin C, 3.5 to 4.5 parts of vitamin B1, 2 to 3 parts of vitamin B2, 2.5 to 3.5 parts of calcium pantothenate, and 1.5 to 2.5 parts of vitamin B6. A preparation method of the composition comprises the following steps of: uniformly stirring the components in a mixer; putting the components into a full-automatic capsule filling machine; and performing the process steps of capsule sowing, capsule separating, filling and capsule locking to obtain an encapsulated composition. The composition can be used for the prevention, treatment or auxiliary treatment of the cardiovascular and cerebrovascular diseases or chronic diseases.
CA2117638C Adhesive bandages, wound dressings, sutures, drapes, orthodontic rubber bands, toothbrushes, and the like An adhesive bandage, wound dressing, suture-like mechanism, or surgical drape for use over a wound is made from a laminate structure of flexible rubber, a hydrophilic hydrogel polymer bonded to one side of the flexible rubber, and an adhesive bonded to the hydrophilic hydrogel polymer along at least a first section of the adhesive bandage, wound dressing, suture-like mechanism, or surgical drape. The adhesive is preferably a hydrogel adhesive with a cellulosic, polyurethane or polyacrylate base, while the flexible rubber is preferably rubber which is pretreated with hydrogel polymer prior to curing. A medicament such as CPC or BAK can be bonded to the hydrophilic hydrogel polymer along the non-adhesive portion of the adhesive bandage, wound dressing or surgical drape to provide slow release medication, and if desired, movable plastic may be provided to cover the adhesive portions. In one embodiment, the adhesive bandage (10) is a laminate comprised of a flexible elastomer (15) to which on one side is bonded a hydrogel polymer coating (20). An adhesive (25) is bonded to at least certain sections of hydrogel polymer coating (20).
CN1768741A Instant release type orally administered medicinal composition The invention relates to the instant release type oral medicinal composition containing the calcium salts or hydrates of benzyl succinate derivatives represented by formula (I) as the active constituent and can be used as medicament for treating diabetes.
US7145037 Adamantane derivatives with neuroprotective, antidepressant and anti-ischaemic activities, and process for preparing them The invention describes compounds represented by the general formula (I) given below: in which: n is an integer between 1 and 4; R1 and R2 are chosen independently from hydrogen and a methyl group; R3 is chosen independently from a linear, branched or cyclic alkyl group containing from 1 to 3 carbon atoms (R3a) and a simple amino group (R3b) or an amino group substituted with a nitro group (R3c) The compounds are useful for treating central nervous system diseases or peripheral neuropathies.
US7465443 Acellular antibordetella vaccine The invention relates to an immunogenic composition, characterized in that it comprises an adenyl cyclase-hemolysin (AC-Hly) protein, or an immunogenic portion of this AC-Hly, of a strain of Bordetella chosen from B. pertussis, B. parapertussis or B. bronchiseptica, and in that it comprises, in addition, a bacterial extract containing the expression products of the vrg genes of a strain of Bordetella chosen from B. pertussis, B. parapertussis or B. bronchiseptica, or a portion of these expression products which is sufficient to induce an immune response in a host to which the extract might be administered.
CN101244106A Yacon antidiabetic extract and preparation method The invention discloses a Yacon antidiabetic extraction, which is characterized in that the weight percentage of smallanthus sonchifolius diterpenoid acid which comprises the general formula (I) is 0.1 to 100 percent. The preparation method of the Yacon antidiabetic extraction comprises the following steps: first, use water or low-concentration ethanol to extract Yacon leaf and get Yacon leaf concentrated extractant via concentration; next, use water or/and low-concentration ethanol first and then high-concentration ethanol to elute the macroporous resin column on Yacon leaf concentrated extractant to collect high-concentration ethanol eluate; then, concentrate the high-concentration ethanol eluate via reduced pressure; finally, dry and refine. The extraction has the advantages of good antidiabetic function proven in vitro test so as to be used for preparing the antidiabetic medicine and easy preparation method, thus being suitable for industrial production.
CN101904864A Application of silicone oil in preparing allergen retarder The invention relates to an application of silicone oil in preparing an allergen retarder. Silicone oil can be smeared on the inner wall of the nasal cavity to stick allergens in the air to inhibit the allergic reaction, thereby performing the functions of preventing and relieving the allergic rhinitis. The inventor discovers that when the silicone oil is used before the stage of attack of the seasonal allergic rhinitis, the attack of the seasonal allergic rhinitis can be effectively prevented; after the attack of the seasonal allergic rhinitis, a patient continuously uses the silicone oil for two weeks, and then, the attack degree of the seasonal allergic rhinitis can be effectively relieved; and for perennial allergic rhinitis, the patient continuously uses the silicone oil for two weeks, and then, the attack degree of the perennial allergic rhinitis can also be effectively relieved.
WO2013015634A3 Pharmaceutical composition for treating atopic dermatitis A method of treating mild atopic dermatitis patients by locally administering an external composition containing adenosylcobalamin as an active ingredient is provided. The composition can effectively treat mild atopic dermatitis patients without side effects.
CN102379839A Preparation method of salicylic acid ointment The invention discloses a preparation method of a salicylic acid ointment, and the product belongs to the field of pharmacy. The product takes salicylic acid crystal, dimethyl sulfoxide, sorbitan fatty acid ester-80 and vaseline as raw materials, and is successfully prepared through a certain technology. The production process of the product is pollution free, the produced salicylic acid ointment particle is fine and smooth, the salicylic acid content in the product is 1.5%-15%, and accordingly, the product can be applicable to the treatment of various skin diseases.
CA2106613C Benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them The invention relates to benzoylguanidines of the formula I (see formula I) where R(1) or R(2) ins R(3)-S(O)n- or R(4)R(5)N-O2S- and the other substituent R(1) or R(2) in each case is H, OH, F, Cl, Br, I, alkyl, alkoxy, benzyloxy or phenoxy, R(3)-S(O)n or R(4)R(5)N- or 3,4-dehydropiperidine and R(3) is alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(4) and R(5) are alkyl or phenylalkyl or phenyl, and in which R(4) and R(5) can also together be a C4-C7-chain, and in which R(4) and R(5), together with the nitrogen atom to which they are bonded, can be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system, and where n is zero, 1 or 2 and their pharmaceutically tolerable salts are excellent antiarrhythmics. They are obtained by a process in which compounds of the formula II (see formula II) in which X is a leaving group which can be easily substituted nucleophilically, are reacted with guanidine.
CN103356665A Application of new mangiferin to prevention and treatment of diabetic nephropathy The invention provides an application of new mangiferin to prevention and treatment of diabetic nephropathy. A plurality of pharmacology experiments prove that the new mangiferin can correct redox unbalance, inhibit generation and aggregation of AGE (Advanced Glycation End Product), inhibit activity of a polyhydric alcohol loop and regulate lipid metabolism so as to resist development of diabetic nephropathy and improve the renal function. Therefore, the new mangiferin has a prospect of treating diabetic nephropathy.
CN101759722A Novel acyclic nucleoside phosphonate predrug The present invention provides a novel R-PMPA predrug as shown in formula I and various medical salts thereof. Meanwhile, the present invention also relates to a medical composition using the compounds as active ingredients and an application of the medical composition as an antiviral drug, particularly a drug for treating and preventing hepatitis B and AIDS viruses.
WO2012046132A1 Quinazoline compounds as sodium channel blockers The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R1-R4 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
WO2007120752A3 4, 5-dihydro- [1, 2, 4] triazolo [4, 3-f] pteridines as protein kinase plk1 inhibitors for the treatment of proliferative disorders The present invention relates to compounds of formula (I) useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
CN102600128A Epigallocatechin gallate medicament and application thereof The invention provides an enpigallocatechin gallate medicament, which consists of 1-49 weight parts of epigallocatechin gallate and 100 volume parts of solvent. The solvent includes but not limited to glucose solution, isoosmotic electrolyte solution, dextran, plasma substitute, water for injection, acetone solution or dimethyl sulfoxide. Dosage forms of the medicament include but not limited to externally applied solution, lotion and patch; ear drops, mouth wash and emulsion; ointment, suppository and aerosol; and spray and aerosol or powder aerosol. The medicament provided by the invention is used for preventing and treating radioactive skin and mucosal injuries, can reduce the occurrence rate of the radioactive skin and mucosal injuries to enable tumor radiotherapy patients to better bear radiotherapy, increase radiotherapy dosage for the tumor and reduce rumor relapse and transfer rate, so that the life time of tumor patients can be prolonged, the survival rate of the tumor patients can be increased, and the living quality of the patients can be improved.
EP1011637B1 Modulation of drug loading in multivesicular liposomes Disclosed is a method for making liposomes, for example multivesicular liposomes (MVLs), containing one or more biologically active agents, wherein the loading of the active agents into the liposomes is modulated by adjusting the osmolarity of the aqueous component into which the agents are dissolved prior to encapsulation. To increase the loading of the active agent, the osmolarity of the aqueous component is reduced, and to decrease the loading of the active agent, the osmolarity of the aqueous component is increased. In the making of MVLs, the process involves dissolving the active agent and an optimal osmotic excipient in a first aqueous component encapsulated within the liposomes. For any given concentration of drug, the osmolarity of the first aqueous component can be adjusted by increasing or decreasing the concentration or molecular weight of the osmotic excipients used therein. The rate of release of the active agent into the surrounding environment in which the liposomes are introduced can be simultaneously controlled by incorporating into the lipid component used in the formulation at least one long chain amphipathic lipid. For example the amphipathic lipid can have from about 13 to about 28 carbons for example, from about 18 to about 22 carbons, in its carbon chain. Use of the long chain amphipathic lipid in the lipid component is particularly helpful in controlling the release rate and encapsulation efficiency for high drug load formulations.
WO2009047303A2 Metabotropic glutamate receptor modulators for the treatment of pervasive developmental disorder The invention concerns the use an mGluR modulator, e.g. an mGluR5 modulator, for the treatment, prevention or delay of progression of a pervasive developmental disorder. The invention further concerns the use of an mGluR modulator for the treatment, prevention or delay of progression of a disorder is selected from Fragile X syndrome and fragile X- associated tremor/ataxia syndrome (FXTAS).
CN101757018A Polyinosinic powder for livestock and preparation method thereof The invention aims to provide veterinary polyinosinic powder which mainly comprises poly cytidine acid, poly inosinic acid and auxiliary material, is prepared through a series of processes, such as mixing, dissolving, granulating, drying, grinding and the like, and is mainly used to prevent and treat the virus diseases of the livestock. Through the clinical therapeutic effect test we find that the medicine is characterized by good therapeutic effect, little dosage and high efficiency in preventing and treating the virus diseases of the livestock, and is suitable to be popularized and applied in the livestock industry.
CN102070432A Novel preparation method for hypocrellin B serving as photosensitizer The invention discloses a novel preparation method for hypocrellin B serving as a photosensitizer. The method comprises the following steps of: separating crude extract out from hypocrellin by a water bath lock type reflux method; and separating by a silica gel column chromatography to obtain the hypocrellin B. The method is easily and efficiently operated; a hypocrellin B single product can be effectively separated; and a better basis is provided for the development of the hypocrellin B.
US20090318546 Chromen-2-One Derivatives A compound of formula (I) wherein R1, R2, R3, R4, R5, and ring A are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
CN101088510B Use of Cordycepic polysaccharide in pharmacy The present invention relates to the medicine use of cordycepic cefopolysaccharide, and reveals medicine of cordycepic cefopolysaccharide for preventing and treating acute and chronic renal failure and renal drug toxicity. Cordycepic cefopolysaccharide is extracted from cordycepic powder through water extraction and alcohol precipitation. Cordycepic cefopolysaccharide contains polysaccharide, including glucose, mannose, galactose, etc, in over 60 wt% and weight average molecular weight of 5-40 KD. Clinically, cordycepic cefopolysaccharide is prepared into medicine alone or together with othermedicine components and in oral preparation forms normally.
CN102388050A N-[(6-azabicyclo[3.2.1]oct-1-yl)-aryl-methyl]-benzamide derivatives, preparation thereof, and therapeutic use thereof The invention relates to N-[(6-azabicyclo[3.2.1]oct-1-yl)-aryl-methyl]-benzamide derivatives of the general formula (I) where: R is a hydrogen atom or a (C1-C6)alkyl group, (C3-C7)-cycloalkyl, optionally substituted by one or more fluorine, (C3-C7)-cycloalkyl, (C2-C4)alkenyl, phenyl, (C1-C6)alkoxy, hydroxy; R2 is phenyl or naphtyl optionally substituted by one or more halogen, (C1-C6)alkyl, (C1-C6)alkoxy, halo-(C1C6)alkyl, NR4R5, (C1-C6)alkylthio, (C1-C6)alkyl-SO2, phenyl or heteroaryl,; R2 is one or more hydrogen or halogen atom, halo-(C1-C6)alkyl, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)alkyl; R3, R4 and R5 are independently a hydrogen atom or a (C1-C6)alkyl group; R6 is a (C1-C6)alkyl group; R4 and R5 may form together a ring selected from azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, azepine, optionally substituted by a (C1-C6)alkyl group. The invention also relates to the therapeutic use thereof and to a method for synthesizing same.
CN101244037A High concentration middle/long fatty milk injection for injection and preparing method thereof The invention relates to a high-concentration medium/long chained fat emulsion injection for injection. The technical proposal is that the components of the injection comprise 135-165g/l long chained triglyceride (soybean oil, for injection), 135-165g/l medium chained triglyceride (for injection), 11-14g/l lecithin (for injection), 15-25g/l glycerol (for injection), a right amount of sodium hydroxide or eunatrol, and the rest being water for injection. The manufacturing method of the medium/long chained fat emulsion is characterized in comprising steps of fat phase preparation, aqueous phase preparation, foremilk preparation, PH value adjustment, high-pressure homogenization, nitrogen-filled bulking and rotating sterilization. The high-concentration medium/long chained fat emulsion injection has the advantages that the invention provides the medium/long chained fat emulsion injection with safety, high energy, low capacity, isotonicity, low PL/TG ratio for patients; and the invention is suitable for the patients who cannot well utilize the long chained triglyceride due to the lack or inactivity of novain enzyme caused by pathological state and more suitable for the patients who need high energy but contemporarily need restriction on the liquid input.
WO2013049859A1 Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors This invention relates to methods and compositions for treating pancreatic cancer. More specifically, this invention relates to treating pancreatic cancer with certain ATR inhibitors in combination with gemcitabine and/or radiation therapy. This invention also relates to methods and compositions for treating non- small cell lung cancer. More specifically, this invention relates to treating non-small cell lung cancer with an ATR inhibitor in combination with cisplatin or carboplatin, etoposide, and ionizing radiation.
CN1785194A Method for quality control of dioxyl promazine hydrochloride benproperine prepn. A quality control method for dioxopromethazine benproperine hydrochloride includes such steps as examining its characteristics, checking content uniformity and solubility, identification by spectrophotometry and ammonium molybdate depositing reaction, and measuring the contents of dioxopromethazine hydrochloride and benproperine phosphate.
CN103417966A Hydrochloric acid aminolevulinic acid liniment and preparation technology thereof The invention belongs to the medical technology filed and discloses a hydrochloric acid aminolevulinic acid liniment which is composed of a powder agent and a solvent. When the hydrochloric acid aminolevulinic acid liniment is used, the powder agent and the solvent are dissolved by matching with each other. The invention further discloses a preparation method of the hydrochloric acid aminolevulinic acid liniment. The prepared hydrochloric acid aminolevulinic acid liniment is good in effect of treating acne, free of toxic side effects, simple in manufacturing method and wide in application prospect.
CA2364245C Water soluble group ia and iia double metal salt of(-)- hydroxycitric acid This invention relates to a water soluble group IA and group IIA double metal salt of (-)-hydroxycitric acid having the general formula I: (see formula I) The present invention is also directed to a process for preparing the water soluble group IA and IIA double metal salt of (-)-hydroxycitric acid, and the use thereof in beverages and other food products.
CN103349647A Tamoxifen citrate sustained-release granules The invention relates to tamoxifen citrate sustained-release granules, the preparation method of which comprises the steps of preparing tamoxifen citrates into clathrate compounds and further preparing the clathrate compounds into sustained-release granules.
US20110039821 Fused Phenyl Amido Heterocyclic Compounds The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).
EP2646439A1 Alkyl amides as hiv attachment inhibitors Compounds of Formula (I), including pharmaceutically acceptable salts thereof, wherein A is selected from the group (II), are useful as HIV attachment inhibitors.
CN102397231A Itching-relieving and skin-moisturizing soaking bath paste The invention relates to the technical field of a bath supply and discloses an itching-relieving and skin-moisturizing soaking bath paste. A preparation process of the itching-relieving and skin-moisturizing soaking bath paste comprises the following steps of: preparing the following formula medicaments in percentage by weight: 2 percent of ginseng extract, 2 percent of lucid ganoderma, 4 percent of twotooth achyranthes root, 5 percent of divaricate saposhnikovia root, 4 percent of rhizoma atractylodis, 7 percent of sinkiang arnebia root, 3 percent of angelica, 3 percent of medcinal evodia fruit, 4 percent of ephedra, 3 percent of pawpaw, 1 percent of ginkgo and 1 percent of lotus leaf; soaking the formula medicaments by mixing the formula medicaments withand millet wine for two times; combining the medical solution which is prepared by soaking the formula medicaments in the millet wine for two times; uniformly mixing the medical solution; decocting the residue of the medicinal materials in water for two times; combining the decoction which is prepared by decocting the residue of the medicinal materials in water for two times; uniformly mixing the decoction; cooling the decoction until the temperature of the decoction reaches room temperature; adding ethanol of which the concentration is 95 percent into the decoction; uniformly mixing the decoction withand the ethanol; after standing the mixture for 28 to 36 hours, filtering the mixture and performing water extraction and alcohol precipitation; uniformly mixing the supernatant fluid withand the medical solution which is prepared by soaking the formula medicaments in the millet wine for two times; concentrating the medical solution by heating the medical solution until the medical solution becomes pasty; adding 20 percent of deep-sea minerals, 10 percent of deep-sea seaweed, 3 percent of rose essential oil, 5 percent of aloe vera gel, 1 percent of borneol and a proper amount of rice vinegar into the paste; uniformly mixing the added materials withand the paste; filling the mixture into bottles; and vacuumizing and sealing the bottles. The itching-relieving and skin-moisturizing soaking bath paste is clean, health-care and bacteriocidal, is convenient to use, can relieve itching and moisturize skin, promote blood circulation to remove meridian obstruction, and nourish Yin and generate body fluid, and is widely applied to the prevention of skin itching of various symptoms.
WO2012066486A1 Compound ethyl 8-oxo-9-[3-(1h-benzimidazol-2-yloxy)phenyl]-4,5,6,7,8,9-hexahydro-2h-pyrrolo[3,4-b]quinoline-3-carboxylate, salt, crystalline form, cocrystal, formulation, processes for preparation, application as medicaments, pharmaceutical compositions and new use particularly as inhibitor of aurora kinases The invention relates more particularly to a new salt, cocrystal and formulations of ethyl 8-oxo-9-[3-(1H-benzimidazol-2-yloxy)phenyl]-4,5,6,7,8,9-hexahydro-2H- pyrrolo[3,4-b]quinoline-3-carboxylate of formula (F) to preparations thereof and to the use thereof therapeutically, particularly as selective inhibitors of Aurora A and B kinases, and for their use as anti-cancer agents.
WO2009063171A1 Novel rotigotine salts The present invention relates to new salts of N,N-disubstituted aminotetralins, such as rotigotine hydrobromide p-toluenesulfonate, heminaphthalene-l,5-disulfonate, tartrate, and phosphate. Also provided herein are methods of making the new salts and using them for the treatment of diseases that may be prevented, ameliorated or eliminated by the administration of a dopamine D2 receptor agonist or an antiparkinsonian agent.
WO2014020344A1 Compounds and their effects on appetite control and insulin sensitivity The invention provides a propionate inulin ester for the reduction of appetite, food intake and/or calorie intake and/or to improve insulin sensitivity in a subject, and for the treatment or prevention of obesity or diabetes. The invention also provides compositions comprising a propionate inulin ester, methods using propionate inulin esters, functional food containing propionate inulin ester and methods of making propionate inulin esters.
CN102688322A Growth promoting agent for blackone chicken and preparation method thereof The invention discloses a growth promoting agent for blackone chicken and a preparation method of the growth promoting agent and belongs to the technical field of agricultural products. The growth promoting agent is composed of the following ingredients in percentage by weight: 5-20% of liquorice, 5-10% of acontum fischeri, 10-20% of purslane, 5-15% of kudzu root, 5-10% of dried old orange peel, 5-15% of balloon-flower root and 10-65% of calcium carbonate. The growth promoting agent can effectively promote the growth speed of poultry and improve the immunity of chickens.
CN1911306A Ointment for treating beri-beri A medicine in the form of ointment for treating beriberi is prepared from dittany bark, schizonepeta, VB2 and griseofulvin through pulverizing, proportional mixing and adding tooth-paste.
CN101503453A Nucleic acid molecule CRYL1SI3 and use thereof in anti-cancer medicine preparation The invention belongs to the field of biological medicine and relates to a nucleotide molecule and the application thereof in the preparation of antineoplastic medicine. The invention provides a nucleotide molecule used for preparing the antineoplastic medicine, which has the activity of promoting tumour cell to die and the sequence including 5'-GGAAUGUGUUCCAGAAGAU-3' or 5'-GGAATGTGTTCCAGAAGAT-3'. The nucleotide molecule is called as CRYL1SI3. The nucleotide molecule CRYL1SI3 can be combined with daunomycin for use, so as to greatly reduce the drug resistance of the tumor cell.
WO2010038434A1 Process for production of optically active hexahydropyrroloquinoline and intermediate for the process A process for producing a compound represented by formula (IX) [wherein the ring A represents a benzene ring which may have a substituent; G represents a C1-4 alkyl group which may be substituted by a fluorine; and the ring B represents a benzene ring which may have a substituent] or a salt thereof, which is characterized by comprising fusing a compound represented by formula (VII) [wherein each symbol is as defined above] or a salt thereof with an aniline derivative represented by formula (VIII) [wherein each symbol is as defined above] or a salt thereof.
WO2009106516A1 Compositions, kits and methods for a titration schedule for pardoprunox compounds The present invention is directed to compositions, kits, and methods for a titration schedule to facilitate the treatment of a central nervous system condition or disorder by administering a plurality of dosage units of a composition comprising a compound 7-(4-methyl)-1-piperazinyl-2(3H)-benzoxazolone (INN pardoprunox).
US20090220538 vaccine for staphylococcal infections The present invention describes method of preparation and use of polypeptide vaccine formulation for prevention and control of Staphylococci mediated infections in human, bovine and other mammals, using recombinant DNA technology.
EP2776043A1 Biomarkers of response to proteasome inhibitors Disclosed are markers associated with sensitivity to treatment with proteasome inhibitors. Sensitivity is observed when RAS gene is wild type in tumor cells. Compositions and methods are further provided to assess markers of marker genes to predict outcome of treatment using proteasome inhibitors to patients having a solid tumor, such as a lung tumor or a colon tumor.
CN101220100A Separation and purification method for squash polyoses and use of obtained component The invention relates to the technology of extracting three pumpkin polysaccharide components of 50 percent of ethanol precipitate, 70 percent of ethanol precipitate and 80 percent of ethanol precipitate from the pumpkins by means of separating technology by hot water dissolving and ethanol precipitation, which has the following steps: acquiring the pumpkin liquid extract and the organic solvent deposit by hot water extraction, dissolving the deposit by water and condensing the supernatant, removing the protein and obtaining the three pumpkin polysaccharide components of 50 percent of the ethanol precipitate, 70 percent of the ethanol precipitate and 80 percent of the ethanol precipitate via ethanol precipitation. The invention method is simple in technique and suitable for industrial production. The biological activity test shows that the three polysaccharide components have no side effects; the polysaccharide components of 50 percent of the ethanol precipitate and 70 percent of the ethanol precipitate can inhibit the isolated rat islets Beta cell withering and protecting the damaged isolated rat islets Beta cell, while the 80 percent of the ethanol precipitate can inhibit the proliferation in leukemia cell and inducing the withering and differentiation of the leukemia cells.
US20100317682 Single Dosage Unit Including Opioid and Methylnaltrexone or Methylnaltrexone Salt The use of methylnaltrexone bromide in combination and in one dosage unit, with any opioid drug in order to prevent the constipation which can be associated with opioids.
US20090105190 Method for Producing Fucoidan, Fucoidan, and Fucoidan-Containing Composition The present invention provides a method for producing high molecular-weight fucoidan, which is expected to be promising as a cosmetic composition or an agent in the field of dermatology, and a high molecular-weight fucoidan-containing composition. A component containing fucoidan having a weight average molecular weight of 1,000,000 to 2,000,000 obtained through the steps of performing hot water extraction of a mozuku alga body of the genus Cladosiphon at pH 6.0 or higher, which ranges from neutral to alkaline, removing low-molecular weight compound through ultrafiltration, and adjusting a final pH to 6.5 or higher is effective as a cosmetic composition or an agent in the field dermatology, and is also excellent in storage stability.
US20120322863 Prevention of and countermeasures against mitochondrial disease The present invention relates to an agent containing L-arginine, 0.2 to 20 parts by weight of L-ascorbic acid per 1 part by weight of L-arginine, and, if desired, at least one selected from the group consisting of ribonucleic acids, ribonucleotides and ribonucleosides. The agent can treat mitochondrial disease which shows a variety of symptoms caused by dysfunction of mitochondria in cells. L-arginine contained in the agent for treating mitochondrial disease of the present invention increases an NO radical level to thereby dilate the arteries. L-ascorbic acid serves to mitigate a harsh taste and acrid feeling accompanied with the intake of L-arginine and eliminate excessive NO radicals.
CN103156819A Benzoic acid alogliptin composition troche and preparation method thereof The invention relates to the field of pharmacy, and discloses a benzoic acid alogliptin composition troche and a preparation method thereof. The effective components of the benzoic acid alogliptin composition troche comprise benzoic acid alogliptin, mannitol, microcrystalline cellulose, croscarmellose sodium, magnesium stearate and 5% hydroxy propyl cellulose aqueous liquor. The synthetic materials are easy to obtain and low in cost. The troche is quick in disintegration speed, high in dissolution rate, good in stability, accurate in dosage and convenient to take and carry. The benzoic acid alogliptin composition troche is simple in step, short in production period, low in production cost and suitable for industrialized application, and the technical process is easy to control,.
CN100998551A Oral cavity quick dissolved film containing civeran, and method for preparing the same An instant oral membrane of loratadine for relaxing allergic rhinitis, chronic urticaria and other allergic dermatopathy is proportionally prepared from loratadine and at least one biologically acceptable polymer chosen from hydroxypropyl methylcellulose, hydroxypropyl cellulose, maltose dextrin and their mixture. Its preparing process is also disclosed.
WO2012052395A1 Isoxazole derivatives used as oestrogen modulators The present invention relates to a substituted isoxazole derivative according to formula (I), wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt, solvate or prodrug thereof. The present invention also relates to a pharmaceutical composition comprising said substituted isoxazole derivatives and to their use as a contraceptive or in therapy, for instance in the treatment or prevention of estrogen-receptor mediated disorders or estrogen-receptor related physiological conditions such as climacteric disorders and osteoporosis.
CN101405281B Inhibitors of the interaction between MDM2 and P53 The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R<1>, R<2>, A and Z have defined meanings.
EP2090169A1 Nucleic acid-degrading agent and method for degradation of nucleic acid The present invention provides an agent for degrading a nucleic acid, which includes ethidium monoazide as an active ingredient, and is useful as an antibacterial agent such as a bactericide or a disinfectant.
CN1850812B Imidazole derivative, and its preparing method and use for pharmaceutical for tubercle bacillus This invention provides general formula (I) standards new imidazole derivative and its pharmacy acceptable salt, R1-R6 seperately stand for aryl group, heteroatom aryl group, alkyl, cycloalkyl or heterocyclic base group. X1 and X2 seperately stand for oxygen atom, sulfur atom or NR6. It has well anti mycobacterium tuberculosis activity.
CN103083282A Novel hydrogel scar patch and its preparation process The invention relates to a novel hydrogel scar patch and its preparation process. The hydrogel scar patch is composed of a support layer, a hydrogel layer and an isolation layer. The scar patch is characterized in that the hydrogel layer consists of the following components by mass: 0.4-3% of a water-soluble high polymer compound Carbomer, 4-8.5% of polyacrylic acid resin, 0.1-1% of polyvinyl alcohol, 0.1-2% of sodium carboxymethyl cellulose, 0.01-0.5% of polyvinyl pyrrolidone, 20-30% of a moisturizing agent, 0.03-0.3% of a cross-linking agent, 0.02-0.3% of EDTA, 0.05-1% of a bacteriostatic agent, 50-70% of deionized water, a proper amount of a pH conditioning agent, and 1-20% of a drug.
US20110251255 Methods and Compositions for Inhibiting the Proliferation of Cancer Cells A method of decreasing the expression of LIM kinase 1 in a cancer cell comprising; providing an oligonucleotide consisting of the sequence of SEQ ID NO: 1; providing a cancer cell comprising an mRNA encoding LIM kinase 1; and introducing the oligonucleotide into the cancer cell, wherein the oligonucleotide decreases the expression of LIM kinase 1 in the cancer cell. The method also provides compositions of an antisense RNA LIM kinase 1 that can be administered to an individual for the purpose of inhibiting a protein kinase pathway and which further comprises methods for treating and monitoring the proliferation and metastasis of cancer cells. A kit may be used in the detection and treatment of cancer.
US20110112097 Substituted imidazoline-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
US20080280899 Cancer; such as 3-({4-[2-(methylthio)-6-phenylpyrido[2,3-d]pyrimidin-7-yl]benzyl}amino)-1-phenylpropan-1-one; serine/threonine kinase (Akt) suppression; increased cellular potency or solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
WO2010116550A1 Method for testing sensitivity of tumor tissue Disclosed is a method for testing the sensitivity of a tumor tissue to a sulfonamide compound. Specifically disclosed is a method for testing the sensitivity of a tumor tissue to a sulfonamide compound, which comprises the steps of measuring Ktarns values in a tumor tissue collected from a subject before and after the sulfonamide compound or an analogue thereof is administered to the subject and analyzing the distribution of the Ktrans values before and after the administration.
US20080153826 substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorder The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
EP1536786A1 Combination of an allosteric inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib This invention provides a combination, comprising an allosteric inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with celecoxib, or a pharmaceutically acceptable salt thereof, or valdecoxib, or a pharmaceutically acceptable salt thereof. This invention also provides a method of treating a disease that is responsive to inhibition of MMP-13 and cyclooxygenase-2, comprising administering to a patient suffering from such a disease the invention combination. This invention also provides a pharmaceutical composition, comprising the invention combination and a pharmaceutically acceptable carrier, diluent, or excipient. The invention combination may also be further combined with other pharmaceutical agents depending on the disease being treated.
WO2006054319A2 Use of chitooligomer formulations to modify abnormal activity of chitinase like proteins The present invention provides a use, a composition and a method for treatment of degenerative disorders or diseases in tissues or such as connective tissue, central nervous system, cardiovascular tissue or the immune system. The composition of the present invention comprises chito-oligomers for reduction of abnormally high expression of chitinase like proteins in patients suffering disorders or diseases associated with connective tissue, central nervous system, cardiovascular tissue or the immune system.
EP2010524A2 S1p receptor modulating compounds The present invention relates to compounds that have activity as SlP receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate SlP receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls.
CN103622919A Tilmicosin phosphate enteric granules and preparation method thereof The invention discloses tilmicosin phosphate enteric granules and a preparation method thereof. The enteric granules comprise 70-80 wt% of elemental granule and 20-30 wt% of coating, wherein the elemental granules are at least prepared from the following components in percentage by mass: 5-40% of tilmicosin phosphate, 30-55% of microcrystalline cellulose, 1-5% of sodium carboxymethyl starch, 26.9-30% of starch, 0.1-1% of surfactant and 2-4% of adhesive; and the coatings are at least prepared from the following components in percentage by mass: 78.9-90.9% of I acrylic resin emulsion, 2.3-7.9% of triethyl citrate and 6.8-13.2% of talcum powder. The coatings are coated outside the tilmicosin phosphate elemental granules, so that the tilmicosin phosphate enteric granules are basically not released in the livestock or fowl stomach, but are gradually and completely released in the livestock or fowl intestinal tract, thereby obviously enhancing the treatment effect of the tilmicosin phosphate.
US20110092595 Compositions and Methods for Treating Lung Cancer Embodiments of the present invention provide compositions and methods for treating lung cancer, including small cell and non-small cell lung cancer that may express HIF-1a by administering a therapeutically effective amount of PX-478.
US20110098300 Compounds Comprising A Cyclobutoxy Group The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals, useful for the treatment and prevention of diseases or pathological conditions of the central nervous system including mild-cognitive impairments, Alzheimer's disease, learning and; memory disorders, cognitive disorders, attention deficit disorder, attention-deficit hyperactivity disorder, Parkinson's disease, schizophrenia, dementia, depression, epilepsy, seizures, convulsions, sleep/wake and arousal/vigilance disorders such as hypersomnia and narcolepsy, pain and/or obesity.
WO2009135449A1 LIGANDS OF ESTROGEN RECEPTORS α AND β, METHOD OF THEIR PREPARATION AND PHARMACEUTICALS COMPRISING THEM The invention relates to novel ligands of the estrogen receptors α and β of general formula (II), which are useful as active substance of pharmaceuticals, for example pharmaceutical compositions useful for hormone replacement therapy, as well as for the treatment of tumour and inflammatory diseases. The invention relates also to a novel preparation method of these ligands comprising cyclotrimerization of ethynylestradiol with the appropriate diyne in an organic solvent. Further, the invention relates to pharmaceuticals comprising the novel compounds according to the invention.
CN102579461A Application of tanshinone IIA in preparation of medicament for treating p53 mutational or deficient tumor The invention relates to the field of natural medicaments, in particular to the application of tanshinone IIA in preparation of a medicament for treating p53 mutational or deficient tumor. The tanshinone IIA can induce cellular poison and apoptosis of p53 mutational H596-NQO1 non-small cell lung cancer cells; and simultaneously, in wild A549 cells of p53, when P53 small interfere ribose nucleic acid (siRNA) silences endogenous P53 genes, the tanshinone IIA can still induce the cellular poison and apoptosis of the A549 cells, reduction in the mitochondrial membrane potential of the A549 cells induced by the tanshinone IIA is not influenced in the process of treating the P53siRNA, the ratio of BAX/Bcl-x1 is increased, cytochrome C is released, and Caspase is activated, so that an anti-tumor effect which does not depend on the p53 is generated.
EP1885372A2 Uses of prostacyclin analogs The present invention provides a method for preventing or reducing the risk of cancer or the progression of premalignant dysplasia in a subject having a higher risk factor by administering a therapeutically effective amount of prostacyclin analog.
US20080249159 Ingesting daily a compound of tetrahydrolipstatin (Orlistat) for a period of at least two years to prevent weight regain; long-term therapy so as to permanently atrophy the endocrine cells which would otherwise generate more ghrelin; appetite reduction A method of reducing ghrelin levels in a human body for weight reduction and to permanently reduce appetite and eliminate weight regain by the step of orally ingesting tetrahydrolipstatin—THL (Orlistat) on a regular basis for a period of at least one to two years.
US20080146502 method for modulating the sensation of satiety perception and to agents useful for same. Such agents are useful in modulating, controlling or otherwise affecting inter alia obesity, anorexia, weight maintenance, metabolic energy levels and/or inflammatory conditions in a subject The invention relates generally to a method for modulating the sensation of satiety perception and to agents useful for same. Such agents are useful in modulating, controlling or otherwise affecting inter alia obesity, anorexia, weight maintenance, metabolic energy levels and/or inflammatory conditions in a subject. More particularly, the invention identifies molecules which interact with ion channels thereby modulating the perception of satiety. The invention contemplates, therefore, a method for modulating the perception of gastric distension by the administration of agents which control the activation or inhibition of mechanoreceptors. The invention further provides compositions comprising these agents and methods of treatment using same. In one embodiment, the invention permits modulation of perception of gastric distension by the administration of agents which control the activation of mechanoreceptors associated with mechanical stretch.
WO2007090134A3 Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma Compositions and methods for treating glaucoma and for treating or preventing retina damage resulting from glaucoma with vanilloid receptor-1 antagonist compounds are disclosed.
US20130195953 Methods and formulations for administration of anti-inflammatory compounds The invention relates to resolvins and their use as anti-inflammatory compounds. The resolvins may be administered in a variety of forms, including drug depots comprising polymers or lipids. The pharmaceutical formulations of the present invention may be used to treat a variety of conditions including acute pain and chronic pain.
CN100575365C Loose knot total polysaccharide and preparation method and usage thereof The invention discloses the oleum terebinthinae total polyoses with a monosaccharide composed of D-Galactose and L-Arabinose. The oleum terebinthinae total polyoses has a good improvement for immunity and a function for anti-tumor and an enhance to the anti-tumor drug such as cyclophosphamide. It not only provides a new treating method to the immunocompromised persons and cancer patients but also points out a new application purpose for enriching the oleum terebinthinae resource. The invention also discloses the prepartion method and applications of the said oleum terebinthinae total polyoses.
WO2014086964A1 New derivatives of indole for the treatment of cancer, viral infections and lung diseases The present invention relates to a new class of indole derivatives, having a particular MKlp2 inhibition profile and useful as a therapeutic agent, in particular for the treatment of cancer, viral infections and lung diseases.
CN103012248A Synthesis of amino combretastatin derivative and application of amino combretastatin derivative as oral antitumour drug The invention discloses a compound which is shown as a formula (I) and used for inhibiting generation of tumour neovascularization as well as officinal salt or a configurational isomer thereof, wherein substituent groups R1, R2 and R3 are defined in the specification. The invention also discloses a preparation method of the compound in the formula (I), a pharmaceutical composition and an application of the compound as a microtubulin inhibitor in the aspect of inhibiting the tumour neovascularization, especially an application as an oral preparation.
WO2005009436A1 Dispersible formulation of an anti-inflammatory agent A method is provided for treatment and/or prevention of an inflammatory condition in a fluid-containing organ having a natural exterior orifice, such as lthe udder of a milk-producing animal or an ear of a subject. The invention also relates to a dispersible pharmaceutical composition suitable for infusion into the organ according to the method of the invention, and a process for preparing such a composition.
CN102807548A Norathyriol crystal I and preparation method thereof The invention discloses a norathyriol crystal I. Results of X-ray powder diffraction analysis, DSC, TG-DTA analysis, IR and HPLC analysis show that the norathyriol crystal I is a new crystal morphology. Compared with the existing norathyriol, the norathyriol crystal I of the present invention has advantages of high purity, light stability, moisture stability, thermal stability, and high oral bioavailability. The invention further provides a preparation method for the norathyriol crystal I, and pharmaceutically-acceptable carriers of the norathyriol crystal I.
US8268351 time-release agents comprising water-swellable matrix cores containing estrogen derivative extracted from animals surrounded by film-forming coatings A pharmaceutical matrix film tablet with controlled release of natural mixtures of conjugated estrogens which have been obtained from the urine of pregnant mares.
CN103520177A Application of compound in preparing medicine for treating nasopharynx cancer The invention discloses an application of a compound in preparing medicine for treating the nasopharynx cancer and belongs to the technical field of medicine novel applications. The compound is Asperterpenols A. According to the application of the compound in preparing the medicine for treating the nasopharynx cancer, in-vitro MTT antineoplastic activity evaluation shows that the Asperterpenols A has the obvious inhibiting effect on growth of the human nasopharynx carcinoma cell strains of HNE1, HNE2, HONE1 and CNE1, and therefore the Asperterpenols A can be used for preparing the medicine for treating the nasopharynx cancer and is good in development and application prospect. The application of the Asperterpenols A in preparing the medicine for treating the nasopharynx cancer is disclosed for the first time, the nasopharynx cancer cell inhibitory activity of the Asperterpenols A is high, and the application has remarkable progress.
CN102558263A Doxifluridine derivative and preparation method and pharmaceutical application thereof The invention relates to a doxifluridine derivative and preparation method and pharmaceutical application thereof, particularly to a compound shown in a formula (I), and a crystal or pharmaceutical salts of the compound, wherein R1 can be =N-OR4 and the like; R2 can be hydrogen, hydroxyl and X; R3 is can be hydrogen, C2-C6 acyl group and the like; R4 can be hydrogen and the like; and X is F, Cl, Br, I and the like. The invention also relates to a preparation method of the compound. The invention further provides an anti-tumour medicine composition containing the compound, and the application of the compound in preparation of an anti-tumour medicine.
CN101220065A Novel scutellarin compounds and uses thereof The invention belongs to medicine technology field, relates to new scutellarin compound and the application of the new scutellarin. The invention precisely relates to the new scutellarin compound for treating the cardiocerebral vascular diseases. The general formula of the hydroxyethyl (hydroxypropyl or hydroxybutyl) scutellarin compound in the invention is (I), in which R4 is H or Alkyl; R1, R2 and R3 are hydroxyethyl (hydroxypropyl or hydroxybutyl) or H, among which at least one of R1, R2 and R3 is the hydroxyethyl (hydroxypropyl or hydroxybutyl). The compound is substantially used in the prevention and treatment of the cardiocerebral vascular diseases, Alzheimer diseases, cerebral infarction, cerebral ischemia and other varied diseases caused by the cerebral ischemia and so on.
CN103622904A Gatifloxacin liposome gel for eyes and preparation method thereof The invention provides gatifloxacin liposome gel for eyes and a preparation method thereof. The gatifloxacin liposome gel for eyes is composed of gatifloxacin, phospholipids, cholesterol, and the cationic liposome and hydrogel base material prepared through octadecylamine. The gel is uniform in particle diameter distribution, excellent in stability, and easy to be combined with a cornea with negative electricity to improve the permeability of the cornea, and can be continuously positioned at eyes for drug release, so that the toxic and side effects of a drug are reduced, and the biological availability of the drug is improved. The preparation method is practicable in process, and controllable in quality, and has a very broad industrial prospect.
CN101088504A Application of theasaponin in preparing externally applied spermicidal contraceptive The present invention discloses new use of theasaponin, and uses theasaponin in external spermicidal contraceptive. Theasaponin in relatively concentration can kill sperm fast, and has certain antibiotic effect, low cost and high safety. The extracorporeal spermicidal experiment and rabbit contraceptive experiment show that theasaponin has lowest spermicidal concentration of 2.27 g/l for 20s and 1.19 g/l for 3 min, and rabbit contraceptive rate of 100 % when the amount is 100 mg and 50 mg.
CA2294788C Therapeutical system for transdermal delivery of levonorgestrel The invention relates to a physically and chemically stable therapeutical transdermal sytem (TTS) for transcutaneous delivery of levonorgestrel alone or further sex steroid hormones also over a long period. The inventive system is characterized in that it has good fixation properties and comprises a matrix containing polymethacrylate-based steroid hormones to be fixed by contact. The invention also relates to a method for producing such a system, advantageously characterized in that it does not contain any solvent and preserves the active agents. The inventive TTS is characterized in that it is physically and chemically stable, has good fixation properties over long periods and delivers across the skin large amounts of active agents per surface unit. One advantage of the inventive method of production is that said active agents are as little exposed to temperature stress as possible, resulting in minimized degradation or decomposition reactions.
US20120040927 Medicinal antifungal and steroid cream incorporating a biopolymer and a process to make it. The present invention is directed to a composition for treating fungal skin infections & skin inflammation, along with skin rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, a corticosteroid and an antifungal active ingredient. It discloses a composition for treating fungal skin infections & skin inflammation, along with skin rejuvenation containing a) a biopolymer in the form of chitosan, b) a combination of active pharmaceutical ingredients (APIs), clotrimazole and hydrocortisone acetate used in treating fungal skin infections & skin inflammations, c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants and d) water. The active ingredients, namely chitosan, corticosteroid in the form of hydrocortisone acetate, and an antifungal agent in the form of clotrimazole, are incorporated in cream base for use in treating fungal skin infections and skin inflammation due to allergy & itching, & wounds on human skin involving contacting human skin with the above identified composition.
CA2242577C Skin-adhering pharmaceutical preparation, in particular transdermal therapeutic system for the release of 17-.beta.-estradiol to the human organism A pharmaceutical preparation adhering to the skin, in particular a TTS, for the release of the active substance 17-.beta.-estradiol, the concentration of the estradiol contained therein in dissolved form being between its saturation concentration in equilibrium with a gas phase of less than 10% relative air humidity and its saturation concentration in equilibrium with a gas phase of more than 90%relative air humidity, in all matrix layers and, if present, also in an adhesive layer, characterized in that the estradiol quantity contained in the preparation amounts to at least three times the saturation solubility measured at 95% relative air humidity, and that the air enclosed in the package is adjusted to a relative air humidity between 5% and below 0.5%.
CN103030678A Method for preparing rare ginsenoside from malonyl ginsenoside The invention provides a method for preparing rare ginsenoside from malonyl ginsenoside. The method comprises the following steps: crushing fresh ginseng; performing ultrasonic extraction by using ethanol at room temperature; recovering the solvent under reduced pressure; concentrating into aqueous solution; extracting the aqueous solution by using normal butanol; placing a water layer after extraction into a pressure cooker and cooking; taking out a macroporous resin column on the cooked water layer; eluting by using ethanol; and recovering the ethanol to obtain the rare ginsenoside 20R-Rg3, 20S-Rg3, Rg5 and Rk1. By the method, the malonyl ginsenoside can be transformed into the rare ginsenoside with extremely high medicinal value to the maximum degree. The method is simple and quick in operation, low in cost and high in transformation rate, and provides method guarantee for industrialized production of the rare ginsenoside and preparation of new medicines.
US20080138416 Method and systems for using biopolymer-based beads and hydrogels Compositions comprising biopolymers such as alginates and cell attachment peptides are disclosed. Compositions may optionally further comprise cells. Methods for repairing or treating a tissues and organs with such compositions and systems for providing such compositions to tissues and organs, and methods for delivering desired proteins to individual with such compositions and systems for providing such compositions are also disclosed. In vitro methods of culturing cells are also disclosed.
US20120022035 Polymorphic and Amorphous Salt Forms of Squalamine Dilactate The invention relates to select squalamine salts, methods of their synthesis, their therapeutic use and their advantages relating to manufacturing, product stability and toxicity. More specifically, this application is directed to various forms of the dilactate salt of squalamine and their utility in inhibiting neovascularization and endothelial cell proliferation.
US20080194687 particle obtained by granulating 1-aminomethyl-cyclohexane-acetic acid with polyethylene glycol; antiepileptic agents A gabapentin granulate obtained by granulating gabapentin with PEG having a melting point comprised between 50 and 80° C. and pharmaceutical compositions containing it, are described.
CA2180296C Treatment of arteriosclerosis and xanthoma A combination of one or more HMG-CoA reductase inhibitors (for example pravastatin, lovastatin, simvastatin, fluvastatin, rivastatin or atorvastatin) with one or more insulin sensitizers (for example troglitazone, pioglitazone, englitazone, BRL-49653, 5-(4-{2-[1-(4-2'-pyridylphenyl)ethylideneaminooxy]-ethoxy}benzyl)thiazolidine-2,4-dione, 5-{4-(5-methoxy-3-methylimidazo[5,4-b]pyridin-2-yl-methoxy)benzyl}thiazolidine-2,4-dione or its hydrochloride, 5-[4-(6-methoxy-1-methylbenzimidazol-2-yl-methoxy)benzyl]thiazolidine-2,4-dione, 5-[4-(1-methyl-benzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione and 5-[4-(5-hydroxy-1,4,6,-7-tetramethylbenzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione) exhibits a synergistic effect and is significantly better at preventing and/or treating arteriosclerosis and/or xanthoma than is either of the components of the combination alone.
WO2014124651A1 Pyrrolidine-2-carboxylic acid derivatives as iglur antagonists The present invention relates to compounds of Formula (I), combinations and use thereof for disease therapy, or pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoismers and polymorphs thereof, which are iGlu R inhibitors, and hence are useful in the treatment of psychiatric diseases or neurological disorders or a disease or disorder associated with abnormal activities of iGluR receptors.
WO2008000692A2 Pyrimidine and quinazoline derivatives as modulators of somatostatine receptor activity This invention is concerned with compounds of the formula (I) wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
WO2008149062A1 Buspirone for the treatment of nausea and vomiting Buspirone is useful in the treatment of a condition which is nausea, vomiting, retching or any combination thereof, in a human patient, when administered by a route which avoids first-pass metabolism.
WO2012175591A1 Heterocyclyl aminoimidazopyridazines The present invention relates to heterocyclyl aminoimidazopyridazine compounds of general formula (I) : in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
US20100298423 Nutraceutical composition from garcinia mangostana Pharmaceutical, cosmetic, nutraceutical and dietary compositions derived from Garcinia mangostana are rich in γ-mangostin and other demethylated xanthones. These compositions exhibit potent antioxidative activity and reduce inflammation. These compositions may be used in a method of treating TNF-α, and aP2 mediated disorders. The compositions are prepared by subjecting a hydroalcoholic extract of fruit pericarp (fruit hull) of Garcinia mangostana, wherein said hydroalcoholic extract comprises predominantly α-mangostin, to demethylation in the presence of a Lewis acid, an organic base and a catalyst.
CN101530548A Composition with multiple health-care functions and preparation method thereof The invention provides a composition with multiple health-care functions and a preparation method thereof. The composition has the following raw materials by weight portion: 6 to 12 portions of pilose asiabell root, 6 to 12 portions of Chinese angelica, 2 to 15 portions of barbary wolfberry fruit, 2 to 15 portions of Chinese caterpillar fungus, 6 to 12 portions of radix astragali, 6 to 12 portions of hairy antler, 1 to 9 portions of American ginseng, 2 to 15 portions of tuber fleeceflower root, 5 to 18 portions of longan flesh, 5 to 18 portions of Chinese date flesh, 5 to 20 portions of walnut kernel, 5 to 18 portions of rock sugar, 1 to 15 portions of peach blossom, 1 to 15 portions of lily, 6 to 12 portions of donkey-hide glue, 750 to 8,000 portions of yellow wine, 1 to 9 portions of liquoric root and 2 to 15 portions of black bean. The composition adopts various famous and precious pure natural pollution-free raw materials, and is convenient to take, good in taste, easy in absorption, free from chemicals and artificially synthesized substances. The preparation method can release 18 kinds of amino acids in the composition such as lysine, glycin, arginine and 8 kinds of essential amino acids which cannot be synthesized by human bodies. The composition has high efficacy in nourishing liver and kidney and strengthening haematogenesis.
EP1598352A1 1-Glyoxylamide indolizines for treating cancer Disclosed is a compound represented by Structural Formula (I): Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z1 and Z2 are independently =O, =S, =N-OR12 or =NR12 R1 and R2 are independently -H, an aliphatic group, a substituted aliphatic group, an unsubstituted non-aromatic heterocylic group, a substituted non-aromatic heterocylic group, an aryl group or a substituted aryl group, provided that R1 and R2 are not both -H. Alternatively, -NR1R2, taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, -C(R4R5)-, -N(R4)-, -O-, -S-, -S(O)-, -S(O)2-, -C(=O)-, -C(=O)-N(R4)-, or -N(R4)-C(=O)-. R4 and R5 are independently -H or a substituted or unsubstituted aliphatic group. R12 is -H or a substituted or unsubstituted alkyl group.
EP2217572A1 Isoquinoline modulators of atp-binding cassette transporters Compounds of the present invention, of formula (I) and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette ('ABC') transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ('CFTR'). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
US20130052264 Controlled-release pharmaceutical composition including tamsulosin or pharmaceutically acceptable salts thereof, and oral formulation including the same A controlled-release pharmaceutical composition including first and second groups of microparticles, each of the microparticles including a core including tamsulosin or pharmaceutically acceptable salts thereof, a controlled-release polymer coating layer formed on the core, and an enteric polymer outer layer formed on the controlled-release polymer coating layer, wherein the average thickness of the controlled-release polymer coating layer is different in each of the first and second groups of microparticles, and an oral formulation including the same, are provided. This pharmaceutical composition can easily control the extent of release of an active ingredient depending on changes in pH in the intestinal tract and the release pattern of the active ingredient in the small intestine, thus preventing the active ingredient from being rapidly transferred into the blood to thereby minimize side-effects, and maintaining the effective blood concentration of the active ingredient for a predetermined period of time. Furthermore, this composition can shield the bitter taste of the active ingredient even when exposed to the inside of the mouth, thus increasing the therapeutic effects for patients upon oral administration.
US20100040573 Cationic polymers as thickeners for aqueous and alcoholic compositions The present invention relates to a method for producing polymers by radically polymerizing a mixture comprising 99.99 to 10% by weight of at least one α,β-ethylenically unsaturated compound with at least one cationogenic and/or cationic group per molecule, 0 to less than 25% by weight of at least one monoethylenically unsaturated amide-group-containing compound different from a) and also 0.01 to 5% by weight of a crosslinker using at least two different water-insoluble initiators.
EP1729761A1 Cadasil treatment with cholinesterase inhibitors The invention provides methods for treating and/or preventing cerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy (CADASIL) in a patient in need thereof by administering a therapeutically effective amount of at least one cholinesterase inhibitor. The invention also provides methods for treating and/or preventing neurovascular diseases caused by one or more mutations of the human Notch3 gene by administering a therapeutically effective amount of at least one cholinesterase inhibitor. In one embodiment, the cholinesterase inhibitor is donepezil, a stereoisomer thereof and/or a pharmaceutically acceptable salt thereof. The methods of the invention may further include administering a therapeutically effective amount of an HMG-CoA reductase inhibitor.
WO2009115927A3 Nucleotide analogues with quaternary carbon stereogenic centers and methods of use The present invention comprises compounds useful as antiviral or antitumor agents. The compounds comprise nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moeities with quaternary centers at the 3' position. The nucleotide analogues can be used to inhibit cancer or viruses. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit viruses or tumors and treat, prevent, or inhibit the foregoing diseases.
CN103012200A Compound with beta-secretase inhibition function, preparation method and applications thereof The present invention discloses a compound with a beta-secretase inhibition function, a preparation method and applications thereof. The compound has a structure represented by a formula I and a formula II, wherein in the formula I, X is -CH=CH- or -CH2CH2-, Y is cyano or amidino, and R1 and R2 are C1-C4 linear alkyl, branched alkyl or substituted alkyl, C1-C4 alkylamino, alkoxy or hydrogen, C1-C4 alkylamido, a halogen-substituted group, hydroxyl or hydrogen; in the formula II, X is O or NH or S, Y is cyano or amidino, R1 is C1-C4 linear alkyl, branched alkyl or substituted alkyl, C1-C4 alkylamino or alkoxy, C1-C4 alkylamido, a halogen-substituted group, hydroxyl or hydrogen, and R2 is C1-C2 alkylamino or alkoxy, a halogen-substituted group, hydroxyl or hydrogen. The compound has a good beta-secretase inhibition activity and has broad application values.
CN103749327A Long-haired rabbit shearing method The invention provides a long-haired rabbit shearing method. According to the method, electric clippers are used for shearing, and a long-haired rabbit is injected with accelerant by means of subcutaneous injection 5-25 minutes before shearing; the accelerant includes effective ingredients, including amiphenazole and vitamin B12; 0.1-0.2g of amiphenazole and 0.5-1g of vitamin B12 are applied per kg of rabbit. The accelerant containing pharmaceutically acceptable auxiliary ingredients is prepared into injection for injecting, according to a veterinarilly acceptable proportion. The accelerant has the effects of quickening blood circulation of rabbits and promoting fascicular follicular expansion and takes effect in a few minutes after injecting, specifically follicles can more strongly support rabbit hairs, so that the roots, close to skin, of the rabbit hairs are stiffer and shearing with the electric clippers is facilitated.
WO2011007961A2 Immunostimulatory compositions comprising liposome-encapsulated oligonucleotides and epitpoes The present invention relates to a composition for enhancing an immune response, an epitope having immunogenicity, screening and preparing method thereof, a antibody to peptide antigen and screening and preparing method thereof. The composition of the present invention may be effectively used for preventing or treating diverse immune-deficiency diseases such as cancer, influenza virus, hepatitis C virus and RSV (respiratory syncytial virus) by enhancing immune responses.
EP1910297A1 Isoquinoline compounds Isoquinoline compounds are provided that influence, inhibit or reduce the action of a G-protein receptor kinase . Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
US20080194661 1-(5-(4-trifluoromethyl-benzylamino)-1H-indazol-1-yl)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol; 2-(2,4-difluorophenyl)-1-(1H-indazol-1-yl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same.
WO2009124399A1 Inhibition of cell migration by a farnesylated dibenzodiazepinone The invention relates to the discovery that dibenzodiazepinone analogues have cell migration inhibiting activities on neoplastic and endothelial cells. The migration of neoplastic cells from various tumor types, such as a glioma tumor that may comprise an EGF and/or PTEN mutation, or a Ras-, Raf, or EGFR-mediated tumor, may be inhibited when contacted by the dibenzodiazepinone analogues of the present invention. The invention includes methods for inhibiting migration of a cell in a subject, by contacting a cell with a dibenzodiazepinone analogue of the present invention.
US7501441 for treating uterine fibroid disease; [2-(4-hydroxyphenyl)-6-hydroxynaphthalen-1-yl][4-(2-(1-piperidinyl)ethoxy)phenyl]methane; therapy for post manupausal women The present invention is a method for treating uterine fibroid disease using a compound of formula I wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C4-C6 alkyl); R2 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl) or —OSO2(C4-C6 alkyl); n is 2 or 3; and R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof.
CN101610760B Treatment of cachexia The present invention provides a means for prevention and treatment of cachexia and other chronic illnesses including but not limited to the promotion of weight gain, reduction or prevention of weight loss by administration of a substance that both reduces the sensitivity of beta-adrenergic receptors and of 5-HTla receptors. (S)- pindolol, (S)-propranolol, tertatolol or bopindolol are preferred for this purpose.
US20080234343 For oral administration, a transparent liquid mixture of an oily base, a surfactant, polar solvent, and an amount of a drug that is not very soluble in the solvent that exceeds its solubility in the solvent; dugs include 1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide derivatives A composition for oral use, which contains a drug compound (in particular, a hardly water soluble or water-insoluble drug compound) in an elevated amount and is excellent in the absorbability of the drug compound via the digestive tract, is produced by dispersing the drug compound in an oily base and a surfactant in an amount exceeding the solubility thereof in the mixture of the oily base with the surfactant under heating, adding a polar solvent which serves as a poor solvent for the drug compound to the thus obtained dispersion, and heating the mixture to give a transparent liquid composition. Further, the obtained composition is encapsulated to give a capsule preparation.
US20100216821 Benzimidazoles With A Hetero Spiro-Decane Residue As NPY-Y5 Antagonists The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts, solvates, stereoisomers thereof, R1 may be C1-C4 alkyl, aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; R2 may be halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano, nitro; or aryl, heteroaryl or heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R2 may correspond to —O—R3; R3 is a 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen X is carbon or oxygen; Z is carbon or nitrogen; G is a fused 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen; m may be 0 or an integer ranging from 1 to 4; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY-Y5 receptor antagonists.
US20130011485 Magnetic nanomedicine for inhibiting/treating human prostate cancer The present invention discloses a magnetic nanomedicine for inhibiting/treating human prostate cancer, which comprises a core containing a magnetic particle having a diameter of less than 10 nm; a shell made of a carboxylated polyaniline and encapsulating the core; and a medicine covalently linked to the shell and able to inhibit/treat prostate cancer. The magnetic nanomedicine of the present invention not only has superior thermal stability and but also has water solubility higher than that of the conventional anti-prostate cancer medicine. Further, the magnetic nanomedicine of the present invention can be magnetically conducted to the cancer area to increase the local concentration of medicine and enhance the therapeutic effect.
WO2009153665A2 Inhibitors of the shiga toxins trafficking through the retrograde pathway The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.
US20120178757 Method For The Prevention Of Cancer Metastasis A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.
CN1839788A Immune globulin G biological factor oral detergent The invention discloses an immune globulin G biological factor oral detergent which comprises erythritol, oligosaccharide, stachyose, xylitol, trehalose, mentha camphor, peppermint essence, refrigerant alcohol, aspartame, Acesulfame-K, immunoglobulin-G, and water for injection.
US20090048461 Regulators of Bacterial Signalling Pathways The present invention provides a method for the preparation of compounds of formula (II). The invention also provides novel compounds of formula (II) and their use in medical, scientific and/or biological applications.
US20090118335 Acid Secretion Inhibitor The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like. A proton pump inhibitor containing a compound represented by the formula (I) wherein ring A is a saturated or unsaturated 5- or 6-membered ring group optionally having, as a ring-constituting atom besides carbon atom, 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom, ring-constituting atoms X1 and X2 are each a carbon atom or a nitrogen atom, a ring-constituting atom X3 is a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, R1 is an optionally substituted aryl group or an optionally substituted heteroaryl group, R2 is an optionally substituted alkyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group, R3 is an aminomethyl group optionally substituted by 1 or 2 lower alkyl groups, which is a substituent on a ring-constituting atom other than X1, X2 and X3, and ring A optionally further has substituent(s) selected from a lower alkyl group, a halogen atom, a cyano group and an oxo group, or a salt thereof or a prodrug thereof.
US6916926 Process for the preparation of (±) 1-3-dioxolanes and the optical resolution thereof (±) 3-(4-Phenyl-1-piperazinyl)-1,2-propanediol cyclic acetals, a process for the optical resolution thereof and their use as intermediates for the preparation of (−) 3-(4-phenyl-1-piperazinyl)-1,2-propanediol (levodropropizine) and salts thereof are described herein.
US7511075 Therapeutic malonic acid/acetic acid C60 tri-adducts of buckminsterfullerene and methods related thereto Disclosed and claimed herein are e,e,e malonic acid/acetic acid tri-adducts of buckminsterfullerene of the general formula C60R3, wherein each R is independently selected from groups of the formula ═CR1R2 wherein each R1 and R2 is independently selected from the group consisting of —H and —COOH, provided, however, that at least one of the R1's and R2's is a hydrogen. Processes for preparing and uses of the same for treating neuronal injury and for life-extension are also disclosed and claimed herein.
CN102247365A Medical application of compound and medicament preparation thereof The invention discloses a medical application of compound and a preparation thereof, belonging to the technical field of medicaments, in particular to the application of medicine composite of N-(2-methoxy ethyl)-2-(-3-nitro-1,2,4-triazole-1-) acetamide and nitro oxadiazole acetic ether in preparing medicament capable of treating medicament capable for adding sensitive action on radioactive ray bytumor cells. The clinical test proves that 600-1000mg of medicine composite has good hypersensitivity. After the medicine is injected and used, the sensitivity of the tumor cell on the radioactive ray is improved, the effect of irradiation in low dose can achieve the effect of irradiation in high dose, each function of the organism does not lower acutely, and thus the medicament has wide market prospect.
CN103271961A Preparation for treating rheumatic bone diseases The invention relates to a preparation for treating rheumatic bone diseases. The preparation comprises a first pharmaceutical composition and a second pharmaceutical composition, wherein the first pharmaceutical composition comprises substances in parts by weight as follows: realgar, Chinese blister beetles and asarum; and the second pharmaceutical composition comprises substances in parts by weight as follows: pearls, borneol, cinnabar and pseudo-ginseng. The preparation for treating the rheumatic bone diseases has the characteristics that the preparation is low in cost, easy to prepare, insignificant in toxic and side effects and remarkable in curative effect.
CN101683322B Method for preparing nano berberine hydrochloride liposome by supercritical carbon dioxide method The invention discloses a method for preparing nano berberine hydrochloride liposome by a supercritical carbon dioxide method. The invention has the following specific operation steps: 1) forming a film; 2) encapsulating drugs; a) preparing berberine hydrochloride liposome injectable suspension; b) incubating in supercritical carbon dioxide fluid; and 3) after finishing releasing the carbon dioxide incubation, releasing carbon dioxide gas and reducing the system pressure into normal pressure to obtain the product. Compared with the prior art, the invention adopts the supercritical carbon dioxide fluid as a medium to prepare the nano berberine hydrochloride liposome with good monodispersity and high drug encapsulation rate according to the characteristics of even mass transferring and highvelocity and the like of the supercritical carbon dioxide fluid, and controls the dimension of the liposome by regulating and preparing pressure.
CN102961435A Medicinal composition for assisting to reduce blood sugar and preparation method thereof The invention discloses a medicinal composition for assisting to reduce blood sugar and a preparation method thereof. The medicinal composition contains the following components in parts by weight: 29.5 parts of propolis, 30 parts of balsam pear, 25.5 parts of radix astragali and 10 parts of chromium picolinate. The medicinal composition is a granule taking medicinal and edible raw materials as the components. The medicinal composition disclosed by the invention is expected to achieve the effect of assisting to reduce blood sugar and is prepared through a scientific and reasonable production process by taking propolis, balsam pear, radix astragali and chromium picolinate as main raw materials; and the product is definite in function, controllable in quality and safe to take. The preparation method of the medicinal composition is simple, and the preparation process can be finished by conventional equipment.
WO2013147568A1 Aminostyrylbenzofuran derivatives as inhibitors against beta-amyloid fibril formation, and pharmaceutical composition comprising same The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid.
US20110263589 Method for preventing or treating a glucocorticoid receptor-related disease A method of preventing or treating a glucocorticoid receptor-related disease involving administering a therapeutically effective amount of a 1,2-dihydroquinoline compound or a pharmaceutically acceptable salt thereof.
CN101711513A Method for increasing sow ovulation rate and injection thereof The invention relates to a method for increasing sow ovulation rate and injection thereof, belonging to the technical field of agricultural biological products. The method of simultaneously injecting PG (cloprostenol sodium) and PMSG (antostab) or a mixture of PG and PMSG before oestrum, and injecting HCG (chorionic corticotrophin) or LHRH-A3 (luteinizing hormone releasing hormone A3) during oestrum is adopted to promote the ovulation rate of young sows or multiparity sows to be 2-3 times of normal ovulation amount, thus improving reproductive performance of sows and obviously increasing the number of young pigs borne by the sows. The method has stable technology and obvious effect, and can not induce ovarian cyst; by using the method, the same superovulation effect can be achieved on standby sows ay any time before sexual maturity.
WO2012089784A1 Fiber and probiotics for reducing intestinal symptoms related to chronic stress The present invention provides a composition that is suitable to reduce the impact of chronic stress on intestinal symptoms and/or conditions. The composition comprises a probiotic microorganism and soluble fiber. Preferably, the soluble fiber is a low viscosity soluble fiber. The composition is in particular suitable to alleviate abdominal discomfort, abdominal pain, abdominal cramps, and bowel movement disturbances; in as far as these conditions and symptoms are associated with stress.
CN1969838A Micro-ecological preparation for treating moniliasis The invention discloses an external agent and formula of chitose derivant to treat skin and mucosa candida albicans infection, which is characterized by the following: forming chelate through combining partial or all Ag, Zn and Cu ion and carrier chitose molecule; adopting ''multiple target point'' typed coordinating action; mixing natural antioxidant such as essential oil, polyphenol material and so on with high-density alkanoate or hydroxylated acid and surface activator.
CN103080096A Bisaryl (thio)morpholine derivatives as S1P modulators The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) wherein R1 is an aryl substitutent selected from phenyl, pyridyl, pyrimidinyl, biphenyl and naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, -SO2-(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl and -NH-CO-(1-4C)alkyl, or substituted with phenoxy, benzyl, benzyloxy, phenylethyl or morpholinyl, each optionally substituted with (1-4C)alkyl, and (8-10C)bicyclic group, bicyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms or oxo; A is selected from -CO-, -NH-, -O-, -S-, -SO- or -SO2-; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R6 wherein the alkylene group may be substituted with (CH2)2 to form a cyclopropyl moiety or with one or more halogen atoms, or R3 is (3-6C)cycloalkylene-R5 or -CO-CH2-R6, wherein R6 is -OH, -PO3H2, -OPO3H2, -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R5 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is -O-, -S-, -SO- or -SO2-; or a pharmaceutically acceptable salt, a solvate or hydrate thereof, with the proviso that the derivative of formula (I) is not 2-[4-(4-chlorophenoxy)-2-chloro-phenyl]-4-morpholineethanol. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
US7265119 For therapy of nicotine dependency The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.
CN101108181A Method of extracting flavone substance and ellagic acid from pomegranate blossom The invention discloses a method for extracting flavonoid substance and ellagic acid from pomegranate flower, which comprises the following procedures: dip the pomegranate flower in edible ethanol for a while, then take it out and place it on a screen, wash it with deionized water, then dry the pomegranate flower; mix and heat the pomegranate flower and the deionized water according to certain proportion, stir them under constant temperature, stop the heating and place the mixture till stillness, filter the mixture with the screen to get preliminary extraction fluid; filter the residue and repeat the previous procedure to get secondary extraction fluid; mix the preliminary extraction fluid and the second extraction fluid to get mixed extraction fluid; conduct ultrafiltration for the mixed extraction fluid to realize anti-penetration concentration of the acquired filtrate; spray and dry the filtrate to get brownish powder with flavonoid content of 5 to 8 per cent and ellagic acid content of 1 to 1.5 per cent. Therefore, the method, which converts the waste into useful material and greatly enhances the added value and comprehensive utilization rate of agricultural products, has no residual organic solvent, brings no harm and toxic content and complies with the quality and safety authentication requirements for drug and health-improving product.
CN101687007A Composition for prevention and/or treatment of peptic ulcer Disclosed is a composition for effectively preventing and/or treating a peptic ulcer that is not induced by Helicobacter pylori, which has no adverse side effect and is highly safe. Specifically disclosed is a composition for preventing and/or treating a peptic ulcer that is not induced by Helicobacter pylori, which comprises a browning reaction product of a sugar and a protein as an active ingredient.
CN102304081A Green synthesis method for ibuprofen piconol and medicinal preparation thereof The invention discloses a green synthesis method for ibuprofen piconol and a medicinal preparation method thereof and provides a formula process of and a green chemical synthesis method of a medicinal compound, in particular the method for preparing ibuprofen piconol, a medicinal composition prepared by using ibuprofen piconol as an active ingredient, and a new formula of an externally-applied preparation for diminishing inflammation, relieving pain and treating infectious diseases. Compared with the prior art, the method has the advantages that: the technical route is advanced, the technical conditions are reasonable, the use of halogenating agents such as thionyl chloride which produce lots of toxic and harmful gases is avoided, a reactions are replaced by one reaction, the operation is simple, convenient and safe, the reaction yield is high, the reaction conditions are easy to control, the solvent and a dehydration condensation agent can be recycled and reused, the problems of trouble of treatment after a reaction process, serious waste gas, waste water and waste residue pollution and the like in the conventional process are solved from the source, environment pollution is avoided, little waste gas, waste water and water residue are produced, and high implementation value and great social and economic benefit are realized.
US20080300284 sustained release niacin formulation with side effect reduction of liver toxicity and effects on glucose metabolism and uric acid levels An orally administered antihyperlipidemia composition according to the present invention includes from about 250 to about 3000 parts by weight of nicotinic acid, and from about 5 to about 50 parts by weight of hydroxypropyl methylcellulose. Also, a method of treating hyperlipidemia in a hyper lipidemic having a substantially periodic physiological loss of consciousness, includes the steps of forming a composition having an effective antihyperlipidemic amount of nicotinic acid and a time release sustaining amount of a swelling agent. The method also includes the step of orally administering the composition to the hyperlipidemic once per day “nocturnally,” that is in the evening or at night.
CN101816473A Tinea-resistant deodorizing nourishing and health care fragrant shoe The invention discloses a tinea-resistant deodorizing nourishing and health care fragrant shoe, comprising the following raw materials by weight percent: 30-50% of adhesives, 15-42% of nourishing agent, 20-47% of bactericidal agent and 1.2-2.3% of flavoring agent. The tinea-resistant deodorizing nourishing health care fragrant shoe further comprises the following components by weight percent: 8% of royal jelly powders and 5% of aloe glue powders, wherein the adhesive is Bali adhesive, the nourishing agent is aloe mineral crystal, the bactericidal gent is triclosan, and the flavoring agent is lemon flavors and osmanthus fragrans flavors. The ringworm-resistant deodorizing nourishing health care fragrant shoe can lastingly remove such pedopathy as tinea pedis, foot stink, onychomycosis and the like, and has substantial effect without relapse.
US7307084 Gastric secretion inhibiting and excellent gastric and intestinal protective action properties, gastrointestinal disorder The invention relates to cyclic benzimidazoles of formula 1, in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.
CN102580017A Preparation method of stomach ache treating paste The invention relates to a preparation method of stomach ache treating paste. The stomach ache treating paste is prepared by drying clove, costus root, frankincense, Chinese eaglewood, nutgrass galingale rhizome and the like into fine powder, grinding borneol into fine powder, uniformly mixing medicinal powder, cutting ginger and green Chinese onion, stirring into paste, extracting liquid, and mixing into paste together with the medicinal powder. During stomach ache, the paste is filled and applied to a shenque acupuncture point, and is fixed with a compound rubberized fabric. According to the method, the stomach ache treating paste is easy to prepare, is convenient to use, has low cost and quick and lasting curative effect, and is a good method for treating various types of stomach ache.
WO2011089951A1 Prevention/treatment agent for diabetic retinopathy and foodstuff aiming to prevent/treat diabetic retinopathy, ameliorating agent for various symptoms of diabetic retinopathy and foodstuff aiming to ameliorate various symptoms of diabetic retinopathy, and method for determining dosing period of prevention/ameliorating agent for diabetic retinopathy Disclosed are a prevention/treatment agent for diabetic retinopathy characterized by containing lutein; said prevention/treatment agent, an ameliorating agent for an electroretinogram, an apoptosis suppression agent for retinal ganglion cells, a decrease suppression agent for molecules related to neural transmission, an ERK activation suppression agent, or a decrease suppression agent for brain-derived neurotrophic factors for being administered in the initial stage of diabetic retinopathy including simple retinopathy or preproliferative retinopathy; and a method for determining the dosing period of a prevention/ameliorating agent for diabetic retinopathy by means of comparing measured electroretinogram values with normal measured electroretinogram values, or by means of observing changes in the thicknesses of the inner plexiform layer, the inner granular layer, and the ganglion cell layer of the retina using optical coherence tomography.
US20100112089 Peptide compound and use thereof The present invention provides a method for the prophylaxis or treatment of cancer in a mammal, comprising administering a therapeutically effective amount of CBP501, a prodrug thereof or a pharmaceutically acceptable salt thereof to the mammal, wherein CBP501, a prodrug thereof or a pharmaceutically acceptable salt thereof is administered simultaneously with or before administration of a nucleic acid damaging agent.
EP1894917A1 Aryloxy- and arylthioxyacetophenone-type compounds for the treatment of cancer The invention relates to compounds of formula (II) wherein ring A is a phenyl, pyridine, pyrimidine or pyrazine ring, W and X are carbon or nitrogen, Y is oxygen or sulfur, R0 is different from hydrogen, Rx is -(C=O)R1 or cyano; R1 is hydrogen, optionally substituted hydroxy or optionally substituted amino, and the other substituents are as described in the specification. The invention further relates to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (II), to the use of a compounds of formula (II) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (II) or pharmaceutical compositions containing same.
WO2008031358A1 1,2-dihydroxy-3-methyl-9,10-anthraquinone in the manufacture of medicaments for treating cancers The use of 1,2-dihydroxy-3-methyl-9,10-anthraquinone in the manufacture of medicaments for treating cancers. The compound demonstrates inhibition towards liver, colon, lung and stomach cancer cells and phosphokinase Aurora-B. The compound of the present invention can be formulated into anticancer pharmaceutical compositions with pharmaceutically acceptable carriers to suppress the continuous growth of tumors.
US7138383 That retains the high RNA binding affinity of the parent oligonucleotide N3' --> P5' phosphoramidates and exhibits a much higher acid stability; inhibiting human telomerase enzyme activity Oligonucleotides with a novel sugar-phosphate backbone containing at least one internucleoside 3′-NHP(O)(S−)O-5′ linkage, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive thiophosphoramidate oligonucleotides were found to retain the high RNA binding affinity of the parent oligonucleotide N3′→P5′ phosphoramidates and to exhibit a much higher acid stability.
CN102579490A Nano-silver antiviral solution and preparation method thereof The invention discloses a nano-silver antiviral solution and a preparation method thereof. The solution comprises 200-500 mug/ml of metal silver particles, 200-500 mumg/ml of tannic acid and 40-100 mumg/ml of sodium carbonate, wherein the particle diameters of the metal silver particles are 10 nanometers on average. The nano-silver antiviral solution has the advantages of uniform distribution, high stability, high virus resistance in particular for respiratory viruses, influenza viruses, parainfluenza virus adenoviruses and the like, no side effect and high safety. The invention discloses a preparation method of a nano-silver antiviral solution which comprises electronegative colloidal state silver nanoparticles, tannic acid and a stabilizer.
CN103393688A Pharmaceutical composition containing calcium folinate and fluorouracil The invention relates to a pharmaceutical composition containing calcium folinate and fluorouracil, and particularly relates to a combined application package comprising a calcium folinate injection and an injection containing fluorouracil. When the combined application package is in use, the calcium folinate injection is intravenously injected and then the fluorouracil injection is intravenously injected.
CN101849916B Cefpiramide sodium powder injection and preparation method thereof The invention discloses a cefpiramide sodium powder injection and a preparation method thereof. The preparation method comprises the following steps: dissolving cefpiramide sodium powder and sodium benzoate in water for injection; dropwisely adding sodium bicarbonate water solution or hydrochloric acid water solution to regulate the pH value to 6.2-7.2; filtering; and freeze-drying the filtrate to obtain the cefpiramide sodium powder injection. In the invention, cefpiramide sodium powder and sodium benzoate are directly dissolved in water for injection to prepare the powder injection in a slightly acid or neutral environment. Thus, the invention has the advantages of controllable related substances, cost saving, simple technical process and energy saving, and is applicable to industrial production.
US20120294823 Method for preparing silk sericin-PVA scaffold using genipin as crosslinking agent A method for preparing a porous-three-dimensional scaffold good for tissue engineering is described. Sericin forms a three-dimensional scaffold with PVA after freeze-drying having glycerin as a plasticizer and genipin as natural crosslinking agent to help making a strong and stable matrix. Adding glycerin into scaffold gives good uniformity and porosity. Smaller pore sizes and better uniformity are obtained as the concentration of genipin in the scaffold increases. Glycerin retains a high moisture content to allow the presence of water molecule in the matrix structure. Adding genipin results in a higher degree of crosslinking within the scaffold. Crosslinking using genipin is most beneficial in preparing scaffold possesses the best biological and physical properties for wound healing. The present invention describes method for preparing crosslinked matrix whose composition can be appropriately tuned to obtain matrix with desirable characteristics for biological applications.
US7776366 improve fertility in mammals, including humans and stallions, including an oil cake component, glucosamine derivative, an acid, minerals, vitamins, and a food component, gametogenesis A method is provided improving fertility in a mammal using glucosamine based composition. The composition is effective to improve fertility in mammals, including humans and stallions.
WO2008146018A2 Drug delivery system comprising matrix metalloproteinase inhibitors A composition for topical application to a subjects skin comprising a matrix metalloproteinase inhibitor, more particularly an inhibitor selected from the group consisting of : TIMP-I, TIMP-2, TIMP-3, TIMP-4, Ilomastat, MMP inhibitor 111, CL82198, GM1489, and FN-439 is used for the prevention or treatment of soft skeletal tissue extracellular matrix degeneration, more particularly wherein the soft skeletal tissue is a tendon or ligament, and more particularly where the tendon is -selected from the group consisting of : superficial digital flexor tendon (SDFT), suspensory ligament, deep flexor tendon, deep digital flexor tendon (DDFT), accessory ligament of the deep digital flexor tendon, cruciate ligament, Achilles tendon, flexor tendon, quadriceps tendon, rotator cuff, and lateral or medial epichondylitis, and more particularly wherein the musculoskeletal injury or disorder is selected from superficial digital flexor tendinopathy and suspensory ligament desmitis, Achilles tendon injuries, rotator cuff injury, lateral epicondylitis, medial epicondylitis and patellar tendinopathy.
CN1568953A Method for preparing mental disease resistant medicine containing succinic acid The invention discloses a method for preparing a medicament for treating psychoneurosis such as epilepsy, which comprises succinic acid 50%, lactin 20%, crystalline cellulose 22%, calcium carboxymethylcellulose 2%, waterless silicon acid 2%, carboxyl propionyl cellulose 3%, and magnesium stearate 1%.
US20080107599 Radiolabelled benzamide analogues, their synthesis and use in diagnostic imaging Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 18F, can be used as radiotracers for imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labelled with 123I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
CN102250069A Pyrrolic amide compound and purpose thereof in preparation of anti-malignant tumor medicament The invention relates to pyrrolic amide compounds and purposes thereof in preparation of anti-malignant tumor medicaments. The thiazole amide compound of the invention is an ideal tyrosine kinase inhibitor, and can be used in preparation of medicaments for treating malignant tumor, but not limited to indications of renal carcinoma, liver cancer, gastrointestinal stromal tumor and non-small-cell carcinoma, etc.
CN101219994A Ozagrel ester, composition and production method thereof The invention discloses an ozagrel ester with the compounds of the ozagrel ester. The ozagrel ester is provided with a chemical structural formula as listed on the right. The compounds of the ozagrel ester comprise an ozagrel ester with the amount of effective treatment and a carrier accepted in medicine. The invention also discloses the preparation methods for the ozagrel ester and the compounds of the ozagrel ester. The ozagrel ester of the invention has good solubility and stability; besides, the compounds of ozagrel ester can be conveniently made into a plurality of liquid, solid, freeze-drying and mucosa or the skin medication agents.
US20090099099 Isoflavone Glycosides as Peroxisome Proliferator-Activated Receptor-alpha Modulator A method of treating or preventing diseases related to modulation of PPAR-α in comprising administering to a human or other mammals in need of such treatment an effective amount of plant material derived from plants of the genera Puerila Lobata.
CN101780059A Transdermal preparation containing ligustrazine phosphate and preparation method thereof The invention discloses a transdermal preparation containing ligustrazine phosphate and a preparation method thereof. The transdermal preparation containing ligustrazine phosphate comprises a backlining layer, a frame-type medicine reservoir layer, an adhesive layer and a protective layer, wherein, the part of the frame-type medicine reservoir layer is obtained by a composite system of a biopolymer material and sodium alga acid under the cross-linked action of calcium chloride water solution, and comprises the following components in parts by weight: 1-20 parts of ligustrazine phosphate, 75-95 parts of the biopolymer material and sodium alga acid, 0.5-5 parts of calcium chloride and 0.5-10 parts of transdermal accelerator. The invention has buffering and release control functions, thus ensuring durable and stable medicine effect, not causing anaphylaxis and having no toxic reaction.
WO2006114372A1 Acetyl l-carnitine for preventing painful peripheral diabetic neuropathy The use of acetyl L-carnitine, or of one of its pharmaceutically acceptable salts, is described for the preparation of a medicament useful for the prevention of painful peripheral neuropathy in patients suffering from type 2 diabetes, in which said symptoms are selected from the group consisting of pain, paraesthesia and hyperaesthesia, in which the acetyl L-carnitine is administered orally at a dose of at least 3 grams/day.
US20080312339 Fluorine-substituted alkyl phenol compounds and their uses The present invention relates to the synthesis of fluorinated forms of alkyl phenol compounds and their subsequent use as pharmaceutical agents. More specifically, alkyl phenol compounds are fluorinated to increase compound volatility such that the compound may be administered to a mammal, such as a human being, by inhalation. The invention also provides an inhaler (or vaporizer), that can be used for administration of the volatile derivatives of fluorine-substituted alkyl phenol compound. Further, different derivatives of fluorine-substituted alkyl phenol compound can be also administered by other routes as described in this document.
US8524720 Substituted N-(pyrazol-5-yl)-pyrrolo[3,2-D]pyrimidin-4-amine useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2′, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
CN101967135A 4-aryl coumarin compound and preparation method and application thereof The invention discloses a 4-aryl coumarin compound and a preparation method and application thereof. The 4-aryl coumarin compound has a structure shown in a formula (I). The preparation method comprises the following steps: taking substituted benzaldehyde and propandioic acid as raw materials, heating under condition of existing pyridine and piperidine, and generating Perkin reaction and decarboxylic reaction to obtain a series of substituted phenylacrylic acid compounds; carrying out bromination and elimination reaction on the substituted phenylacrylic acid compounds or acetylation to protect a phenolic hydroxyl group, and then carrying out bromination and elimination reaction to obtain substituted phenylpropiolic acid compounds; and enabling the substituted phenyl propargylic acid compounds and phenolic compounds to react under the catalysis of boron trifluoride etherate and phosphorus oxychloride or trifluoroacetic acid to obtain a series of 4-aryl coumarin compounds. The compounds can be used for preparing antineoplastic medicine, anti-abnormal-angiogenesis medicine, antimicrobial medicine, antioxidation medicine and antimalarial medicine.
WO2004087158A3 Muscarinic m1 receptor agonists for pain management Disclosed herein are compounds and methods for treating chronic neuropathic pain. It has been discovered that compounds that selectively interact with a muscarinic receptor subtype are effective in treating neuropathic pain. Specifically, compounds that selectively interact with the M1 muscarinic receptor subtype may be used.
EP2191849A1 Drug for suppressing pathogen occurringin vivo To provide a drug for actively metabolizing or excreting a pathogen occurring in vivo. The present invention is directed to a compound which is formed of (A) an adsorbent for a pathogen occurring in the blood or lymph, and (B) a ligand which is specific to an organ or cells capable of metabolizing or excreting the pathogen and which is bonded to the adsorbent via a linker or with no linker, and to a drug containing the same.
CN103083314A Compound ibuprofen having gastrointestinal protective effect The invention belongs to the field of medicines, in particular to a brand-new compound ibuprofen having a gastrointestinal protective effect. The technical problem to be solved is to provide the compound ibuprofen having the gastrointestinal protective effect; by utilizing the stomach protective effect of nizatidine after taking ibuprofen, gastric side effects of ibuprofen can be improved; the purpose of protecting stomach is achieved; and the compound ibuprofen comprises 15-120 parts of ibuprofen or pharmaceutical salts thereof by weight and 1-40 parts of nizatidine by weight. Furthermore, according to the invention, the technical disadvantages of being easy to degrade nizatidine and poor in stability caused by compatible application of nizatidine and ibuprofen are also overcome; an available solution is provided; and a novel selection for applying ibuprofen safely and effectively in clinical application is provided.
US8722882 Pyrimidine derivatives as GPCR modulators for use in the treatment of obesity and diabetes The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
WO2010050525A1 Compound having tafia inhibitory activity A compound having excellent TAFIa inhibitory activity. Specifically disclosed is a compound represented by formula (I) or a salt thereof. In the formula, A represents a benzene ring or a pyridine ring; X represents -(CH2)-, -(CH2)2-, an oxygen atom, a nitrogen atom or a single bond; Y represents -(CH2)3-NH-R3, -(CH2)4-NH-R3 or a 2-aminopyridyl group; R3 represents a hydrogen atom or the like; R1 represents a hydrogen atom or the like; R2 represents CO2R8, a tetrazolyl group or the like; R8 represents a hydrogen atom, a C1-10 alkyl group or a group having a structure of formula (Ib) or (Ic); and m and n each represents an integer of 0 or 1.
US20070270485 Byrostatin analogues, synthetic methods and uses Biologically active compounds related to the bryostatin family of compounds, having simplified spacer domains and/or improved recognition domains are disclosed, including methods of preparing and utilizing the same.
US20060128810 Remedies for allergic diseases The present invention relates to a prophylactic and/or therapeutic agent for an allergic disease which contains a compound having an agonistic activity to EP3 receptor that is one of the prostaglandin E2 receptor subtypes. More specifically, a compound having an agonistic activity to EP3 receptor is effective in therapy of an allergic respiratory disease such as bronchial asthma, pediatric asthma, allergic asthma, or atopic asthma, and a selective agonistic compound can be expected to induce a more remarkable therapeutic effect.
WO2013017656A1 Antagonists of ribonucleases for treating obesity The present invention relates to antagonists of a Ribonuclease being a member of the RNAse A family for use in treating a disease associated with an increase in adipocyte number or size, such as overweight, or obesity and the like. Also methods for assessing the activity of candidate antagonists of RNAse A family members, uses of cells, tissue or a non-human animal in such screening methods and a kit for carrying out the method are subject of the present invention. Moreover, the present invention relates to agonists of a Ribonuclease being a member of the RNAse A family for use in treating a disease associated with a decrease in adipocyte number. The disease may be lipodystrophy, like hereditary lipodystrophy, drug- induced lipodystrophy, lipodystrophy caused or induced by AIDS/HIV therapy, or traumatic lipodystrophy. The disease may also be is cachexia or a disease associated with disturbed energy storage.
WO2012078915A1 Macrocyclic inhibitors of flaviviridae viruses Provided are compounds of Formula (I): and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
WO2012046945A3 Pharmaceutical and food composition for preventing or treating diabetes or obesity The present invention relates to a pharmaceutical and food composition for preventing or treating diabetes or obesity, and more particularly, to a pharmaceutical composition and functional food for preventing or treating diabetes or obesity and which contain, as active ingredients, novel compounds synthesized from compounds separated from extracts of Stereocaulon alpinum, which is an Antarctic lichen. The novel compounds of the present invention have an excellent activity of inhibiting protein tyrosine phosphatase-1b (PTP-1b), may selectively influence only PTP-1b from among protein tyrosine phosphatases, and may be used as a substantial PTP-1b inhibitor in treating diabetes, and thus may be effectively used in preventing or treating diabetes and obesity.
CN101416980A Use of oligosaccharide in preparing medicine for treating non-bacteria inflammation The invention relates to the application of chitosan oligosaccharide in preparing medicines used for treating nonbacterial inflammations. In the invention, modern separation and purification technologies are applied to the zymolysis of the chitosan oligosaccharide, thereby obtaining the chitosan oligosaccharide with the degree of polymerization ranging from 2 to 50. In addition, intensive study on the effect of neutrophilic granulocytes in inflammations of rats is carried out, and the result shows that the chitosan oligosaccharide has good effect on quickening the death of the neutrophilic granulocytes in inflammations. Therefore, the chitosan oligosaccharide can work as a medicine for treating the inflammations or as a food additive to process and manufacture health care products.
US20120034217 Anti-neoplastic compositions comprising extracts of black cohosh The present invention provides a composition for use in treating or preventing neoplasia, comprising an effective actein. The present invention also provides a composition for use in treating or preventing neoplasia, comprising an effective anti-neoplastic amount of an ethyl acetate extract of black cohosh. The present invention further provides a combination of anti-neoplastic agents, comprising an effective anti-neoplastic amount of an ethyl acetate extract of black cohosh and an effective anti-neoplastic amount of at least one additional chemopreventive or chemotherapeutic agent. Methods for treating and preventing neoplasia are also provided.
US20120004218 Novel tetrahydro-quinoline derivatives A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein A1 to A3 and R1 to R10 have the significance given in claim 1, can be used as a medicament. These compounds are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.
CN101985457A Medicinal salts of cordycepin and preparation method and medicinal application thereof The invention relates to various pharmaceutically acceptable medicinal salts of cordycepin and a preparation method and medicinal application thereof. The invention also provides an application of a medicinal composition which takes various pharmaceutically acceptable medicinal salts of cordycepin as active components for preparing medicines for resisting tumors, medicines for resisting bacteria and viruses, medicines for resisting leukemia and increasing white cells, medicines for regulating immunity, medicines for reducing blood sugar and blood fat, medicines for calming, medicines for resisting inflammation, medicines for resisting renal failure, medicines for relieving asthma and eliminating phlegm, medicines for resisting fatigue and the like.
WO2010059836A1 Substituted aza-bridged bicyclics for cardiovascular and cns disease The invention relates to substituted imidazopyridines, pyrazolotriazinones, triazolopyridines, pyrazolopyridines and pyrazolopyrimidines that are useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I (I) or II (II) in which Cy1 and Cy2 are carbocycles or heterocycles.
CN103550144A Levofloxacin hydrochloride composition injection and preparation method thereof The invention relates to an injection, and discloses a method for preparing a levofloxacin hydrochloride composition injection. The levofloxacin hydrochloride composition injection is prepared through the following raw materials in parts by weight: 50 parts of levofloxacin hydrochloride, 5 to 10 parts of vitamin C, 3 to 5 parts of vitamin B6, and 500 parts of injection water. The method comprises the following steps of (1) fully dissolving levofloxacin hydrochloride, vitamin C and vitamin B6 in injection water; (2) heating the injection water to reach 50 DEG C, adding vermiculite powder and a carbon nano tube, maintaining for 1 to 2 minutes at 50 DEG C, slowly adding to the solution obtained in step (1) along with agitating, and further heating for 5 to 10 minutes; and (3) carbonizing and filtering, adjusting pH (Potential of Hydrogen) to be 4.0 to 5.5, filtering through a millipore filter with aperture less than 0.45 microns, filling, performing moist heat sterilization for 20 minutes at 121 DEG C, detecting the leakage, performing light inspection, and packing to obtain the levofloxacin hydrochloride composition injection. The method has the advantages of good discoloring effect and simple process, and can decrease the content of heavy metal in the levofloxacin hydrochloride composition injection. The vitamin C and vitamin B6 can effectively avoid the degradation of levofloxacin hydrochloride.
WO2009103821A3 Regulators of pb1-f2 activity for treating virus infections The invention relates to means for treating virus infections. It relates in particular to the treatment of influenza A virus infections. Influenza A virus infections include those infections that are caused by virus strains that express the protein PB1-F2. The means for treating virus infections comprise at least one substance that regulates the activity of the protein PB1-F2 as an active component. The invention further relates to vaccines for prophylaxis and/or treatment of virus infections.
US20050085758 Dilute aqueous solution containing epidermal growth factor in gel The present invention features hydrogel drug delivery systems and methods of producing and using such systems for the treatment of wounds. The systems are based on a hydrogel into which a low concentration of growth factor, e.g., epidermal growth factor, is passively transferred from a dilute aqueous solution. When placed in contact with a wounded tissue, the growth factor passively transfers out of the contact lens to provide accelerated healing. The systems are applicable to ocular and other wound treatments.
CN101341145A Isoquinoline aminopyrazole derivatives, their manufacture and use as pharmaceutical agents for the treatment of cancer Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancers.
US20080312193 Substituted Tetracycline Compounds for Treatment of Inflammatory Skin Disorders Methods and compositions for the treatment of skin disorders (e.g., acne, rosacea) are described.
EP2154137A1 Crystalline form of moxifloxacin base Crystalline form of moxifloxacin base of formula (I), a process for its preparation, which comprises the following steps: a) dissolving a suspension of moxifloxacin in an organic solvent which is able to be removed from water, by means of heating to the reflux temperature; b) adding water and cooling to a temperature ranging between 20°C to 40°C; c) removing the organic solvent; d) seeding with moxifloxacin base sesquihydrate; and e) isolating the crystalline form obtained. It is useful for the preparation of pharmaceutical compositions for use as an antibacterial agent.
US20080058371 Bactericides; produces little or no tissue damage or irritation at the injection site An antibacterial formulation suitable for injection into animals containing approximately 2-10% w/v difloxacin HCl, L-arginine base, propylene glycol, ethanol and/or benzyl alcohol, and water. The formulation is a solution having a pH of form 9 to 10. The formulation produces little or no tissue damage or irritation at the injection site.
CN101816694B Echinacea purpurea oral liquid and preparation method and application thereof The invention provides echinacea purpurea oral liquid and a preparation method and application thereof, which can solve the problems of low yield for extraction of an effective ingredient, long extraction time, large using amount of a solvent, high extraction temperature and high degradation of the effective ingredient. The chicoric acid content of the oral liquid is 3 to 30mg/ml; and the echinacea purpurea oral liquid is prepared from echinacea purpurea serving as a raw material by crushing, microwave extraction, filtration, condensation, encapsulation and sterilization. The invention also discloses application of the echinacea purpurea oral liquid in improving the immunity function of animals. The method ensures high yield of the effective ingredient, shortens the extraction time, reduces the extraction temperature, the degradation of the effective ingredient and the using amount of the extraction solvent, improves the production efficiency, saves the production cost and has good application and popularization prospect by taking solution of ethanol with different concentrations as the extraction solvent and using the microwave radiation-assisted extraction.
CN101744910A Anti-computer radiation liniment for external application The invention relates to a health-care product liniment, which is an anti-computer radiation liniment for external application. The liniment is prepared by using almond powder, talcpowder, borneol, musk, egg white and pearl powder as raw materials. The anti-computer radiation liniment for external application of the invention is characterized by simple formulation, rational proportioning, simple manufacturing method and simple and practical use, so that the liniment is particularly suitable for computer users.
US20080234211 Decladinosyl-Macrolides With Anti-Inflammatory Activity The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.
CN1947713A Nano-safflower flavone injection prepn. and its prepn. method A nano-carthamiflavone medicine in the form of liquid injection, powder injection, or perfusion is prepared from carthamiflavone (50-85%) extracted from safflower, medical carrier and medical auxiliary. Its preparing process is also disclosed.
US20090170952 Colchicine compositions and methods Stable ultrapure colchicine compositions comprising ultrapure colchicine and a pharmaceutically acceptable excipient are described. The compositions can be tablets. Methods for preparing such compositions and methods of use are also disclosed. Methods of treating gout flares with colchicine compositions are also disclosed.
CN103626747A N-(2, 3-dihydrobenzofuran-5-yl) benzopyran-4-amide and preparation method and application thereof The invention relates to N-(2, 3-dihydrobenzofuran-5-yl) benzopyran-4-amide shown in a chemical structural formula I, wherein X1-X1 is selected from H, C1-C2 alkyls, C3-C4 straight chain alkyls or branched alkyls, C1-C2 alkoxys, C3-C4 straight chain alkoxys or branched alkoxys, fluorine, chlorine, bromine or iodine; and the invention also provides an application of the N-(2, 3-dihydrobenzofuran-5-yl) benzopyran-4-amide in preparation of anti-cervical cancer drugs.
US8160821 Method for supporting a diagnosis of an effect of a treatment by using anthracycline anticancer drugs and a device for supporting a diagnosis for an effect of a treatment by using anthracycline anticancer drugs A method of supporting a diagnosis of an effect of a treatment by using anthracycline anticancer drugs is disclosed. The method provides a new value for judging an effect, a judgment score, which is calculated based on expression levels and activity values of two cyclin dependent kinases (CDKs). The effect of the treatment by using anthracycline anticancer drugs is judged by comparing the judgment score with a predetermined threshold level.
US20080119491 Amidinoheterocycles as modulators of indoleamine 2,3-dioxygenase The present invention is directed to amidino heterocyclic compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as to pharmaceutical compositions comprising such compounds and to pharmaceutical methods of treatment comprising administration of such compounds and pharmaceutical compositions.
WO2006134963A1 Agent for fibrous disease comprising oxaluric acid derivtive [PROBLEMS] To provide a novel agent for a fibrous disease comprising an oxaluric acid derivative or a pharmaceutically acceptable salt thereof as an active ingredient. [MEANS FOR SOLVING PROBLEMS] The oxaluric acid derivative can significantly prevent the increase in extracellular matrix production induced by TGF-β which plays a dominant role in the fibrillation of various organs and can also inhibit the fibrillation of tissues in a fibrosis model animal. Thus, the compound has an excellent fibrillation-preventive effect, and is therefore highly useful as a prophylactic agent which can prevent the occurrence of various fibrous diseases, i.e., fibrosis and fibrosis-related diseases (e.g., sclerosis), such as pulmonary fibrosis, hepatic fibrosis, nephrosclerosis, myocardial fibrosis, arteriosclerosis and fibrillation diseases in the skin (e.g., scleroderma, keloid) or a therapeutic agent which can prevent the progression of fibrillation in these diseases.
CA2238376C Benzofuran carboxamides and sulphonamides Benzofuran carboxides and sulphonamides have therapeutic utility, e.g, in the treatment of inflammation and asthma, by virtue of their ability to inhibit phosphodiesterases and tumour necrosis factor.
CN1623541A Application of aloelactone in preparation of medicine An application of aloe lactone, 5-(1-hydroxy-2-butenyl)-dihydrofurran-2-one, in preparing the medicines for treating tumor and fungal dermatopathy is disclosed. Its advantage is high curative effect.
CN102813630A Enrofloxacin enteric pellets and preparation method thereof The invention discloses enrofloxacin enteric pellets and a preparation method thereof. The enrofloxacin enteric pellets are prepared from the following raw materials in percentage by mass by wet granulation and pellet coating: 2.5-20% of enrofloxacin, 1-5% of adhesive, 1-5% of disintegrating agent, 15.5-30% of microcrystal cellulose and 40-80% of coating solution. Compared with the prior art, the invention provides enrofloxacin enteric pellets and a preparation method thereof by adopting a pellet preparation technology; the enrofloxacin enteric pellets can perfectly cover the bitter taste of enrofloxacin; and as an enteric sustained-release reagent, the enrofloxacin enteric pellets can avoid the adverse reaction and the like caused by absorption in the stomach. The experimental result indicates that the enrofloxacin enteric pellets provided by the invention have high encapsulation rate and are dissolved out in the intestinal canal environment, the preparation technology is simple, the raw materials are cheap and easily available, and the enrofloxacin enteric pellets are suitable for industrial large-scale production, thus the application prospect is very broad.
US6841679 Acylation of 2-(phenyl)-imidazo(1,2-a)pyridine derivative with oxalyl halide derivative to form anxiolytic agent; reduction, salt formation A compound of the general formula (1), in which: Y denotes hydrogen, a halogen or a C1-4 alkyl group; X1 and X2 denote, independently of each other, hydrogen, a halogen, a C1-4 alkoxy, C1-6 alkyl, CF3, CH3S CH3SO2 or NO2 group; and R1 and R2 denote independently of each other, hydrogen or a C1-5 alkyl group, with the proviso that R1 and R2 do not both denote hydrogen, or a salt thereof, and is prepared by a multi-step process, the last step of which comprises reducing a compound of the general formula (6), in which Y, X1, X2, R1 and R2 are as defined above with an appropriate reducing agent, such as Zn, and, if desired, converting the compound of formula (1) thus obtained, into a salt. The products of this process are known to have useful pharmacological properties, e.g. as anxiolytics.
CN103261413A Marker for determination of sensitivity to triplet combination anti-cancer agent Provided are: a marker for determining the sensitivity to an anti-cancer agent, which can determine the therapeutic reactivity of individual patients; and a novel cancer therapy means which utilizes the marker. A marker for determining the sensitivity to an anti-cancer agent, which comprises at least one gene selected from ALAD gene, C20orf43 gene, CABLES1 gene, CDC14B gene, GDA gene, HOXB6 gene, RPL7AP27 gene, TMEM18 gene and UGT2B10 gene and contains oxaliplatin or a salt thereof, fluorouracil or a salt thereof and levofolinate or a salt thereof.
CN1951463A Medicinal ointment for treating burn and knife wound without leaving scar Disclosed is a medical ointment for treating burn and wound, wherein the formulation comprises (by weight portions) Viola japonica Langsd. 30-50 parts, Pittosporum pentandrum (Blanco) Merr. 20-50 parts, birthwor root 20-50 parts, lead monoxide 1-2 parts. The invention realizes simple process for manufacturing, easiness in use, low cost, and quick relieving pain.
CN101708168A Method for preparing dispersible tablets of tamibarotene The invention discloses a method for preparing dispersible tablets of tamibarotene. The process in the method adopts the solvent deposition method, and the dispersible tablets of tamibarotene, prepared by the method, are good in stability, high in content uniformity and also high in dissolution rate; the method is operated according to the requirements of the Chinese Pharmacopoeia on the dissolution rate of the dispersible tablets, and the dispersible tablets are completely disintegrated within 3 minutes and can pass the No 2 screen(24 meshes), so that the dispersible tablets can enhance the absorption in the human body and improve the biological utilization rate; the preparation method is simple in operation and causes little pollution; by dissolving the tamibarotene in the organic solvents and depositing the tamibarotene in the auxiliary materials, the dust problem in operation can be solved, the caused pollution can be lessened, the untoward reactions of operators are avoided; and the mixed powder of raw materials and auxiliary materials, prepared by the method, can be tabletted directly, so that the cost is saved, and the requirement for being suitable for industrialized production is met.
CN101549083A Chinese materia medica foot bath preserving health essence The present invention relates to a Chinese materia medica foot bath preserving health essence which is prepared from raw materials by weight part as follows: saffron crocus 0.5-1 parts, chuan chinese flowering quince 15-25 parts, lopseed 15-25 parts, yam 10-15 parts, dried rehmannia root 10-15 parts, saussurea involucrata 5-15 parts, american ginseng 5-15 parts, earth poria cocos wolf 15-20 parts,areca-nut 5-15 parts, broom cypress fruit 15-25 parts, Chinese angelica 5-15 parts, and extractum glycyrrhizae liquidum 5-10 parts. The essence has advantages of reasonable prescription, safe use andsimple preparing method which can preserve health and strengthen body. The essence has functions of cleaning deodorizing, stretching muscle and activating collateral, elimination foot fatigue, also has effects of tonifying kidney and boosting liver, benefiting qi and nourishing yin, clearing heat and antitoxic, bactericidal and relieving itching; has obvious assistant treating effect to insomniashort memory, constipated, deficiency body and deficient kidney, waist soreness leg pain, wind dampness bone disease, fungal athlete's foot wet poisonous and menoxenia. The essence integrates treating, preserving and health caring into a whole without fillip and side-effect to human body, and is suitable for general household.
US20090298820 3-substituted-1h-pyrrolo[2,3-b]pyridine and 3-substituted-1h-pyrrolo[3,2-b]pyridine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
US6858629 Heteroaryloxy propanolamines, preparation method and pharmaceutical compositions containing same Compounds of formula (I): where X is N or CH; A represents a group of formula (a) or (b) R1 represents hydrogen or an —NH2, —NR3R4, —NR3CO(C1-C4)Alk or —NR3SO2(C1-C4)Alk group; R2 represents hydrogen, a halogen or a (C1-C4)Alk, (C1-C4)alkoxy, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NR3R4 or —NHSO2(C1-C4)Alk; m and n each represent 0, 1 or 2; R3 and R4 each represent hydrogen or a (C1-C4)Alk group; Y1 and Y2 each represent NH or O; and their salts or solvates, a process for their preparation and the pharmaceutical compositions comprising them.
CN101792444A Sodium levofolinate and preparation method and drug combination thereof The invention provides a method for preparing a sodium levofolinate, the optical purity of the sodium levofolinate is 98.5 percent to 99.9 percent, and the invention also provides the sodium levofolinate prepared by the method and a sodium levofolinate drug combination. The optical purity of the sodium levofolinate prepared by the method can be up to more than 98.5 percent, the obtained sodium levofolinate drug combination is stable in the process of placement, single impurity is less than 0.4 percent, the pH value is stable, the sodium levofolinate has higher safety and a better curative effect when being intravenous administrated.
DE102005059750A1 Use of tetraorganosilicon compound having cell proliferation inhibitory activity, e.g. as an immunstimulator to treat viral-, bacterial- and/or tumor diseases, anemia, arteriosclerosis, arthritis, asthma, autoimmune disease, and cirrhosis Use of tetraorganosilicon compound (I) for the manufacture of a medicament as an immuno-stimulator to treat a specific reaction of the immune system, preferably an inflammation reaction in an organism such as virus, bacteria and degenerated cell inducing pathogen-associated molecular type disease e.g. viral-, bacterial- and/or tumor diseases, where (I) is associated with other compounds such as a substance e.g. nucleic acid binder and -synthesis inhibitor comprising oxoplatin, arsenic-oxide, foscarnet and/or antisense-molecule. Use of tetraorganosilicon compound (I) of formula ((R1>)(R2>)Si(R3>)(R4>)) for the manufacture of a medicament as an immuno-stimulator to treat a specific reaction of the immune system, preferably an inflammation reaction to an organism such as virus, bacteria and degenerated cell inducing pathogen-associated molecular type disease e.g. viral-, bacterial- and/or tumor diseases, where (I) is associated with other compounds such as a substance e.g. nucleic acid binder and -synthesis inhibitor comprising oxoplatin, arsenic-oxide, foscarnet and/or antisense-molecule. R1>-R4>acyloxy of formula (R-COO-) or a peptide of formula (-O-CO-CH(R5>)-N(X)-[CO-CH(R5>)-N(X)]n-CO-CH(R5>)-N(X)2) (both preferred), part of bidendate or multi dentate ligands (by which a chelate complex is formed), alkyl, alkoxy, glucoside or mono-, di- or polysaccarides; R : 5-29C alkyl-, alkenyl- or alkynyl residue (substituted by up to three halo atoms), 1-18C alkoxy or amino group; R5>a different group (i.e. after removing the amino acid group of formula (H2N-CH-COO) in natural amino acid and/or synthetic amino acid), alkyl-, alkenyl-, alkynyl, aryl, heterocycle, cyclic or aliphatic group, a heterocyclic or heteroaliphatic group (optionally substituted by 1-3 of halo, OH, carboxyl, carboxylate, alkoxy or amino), or an ammonium salt (optionally substituted by keto-, aldehyde- or ester groups); X : H or amino protecting group in the peptide chemistry; and n : 0-12. - ACTIVITY : Immunostimulant; Virucide; Antibacterial; Cytostatic; Anti-HIV; Antiseborrheic; Dermatological; Antiallergic; Neuroprotective; Nootropic; Antianemic; Antiarteriosclerotic; Antiarthritic; Antiasthmatic; Immunosuppressive; Analgesic; Hepatotropic; Antidepressant; Antidiabetic; Anabolic; Cardiant; Muscular-Gen; Respiratory-Gen; Antiinflammatory; Osteopathic; Antitubercular; Tuberculostatic; Antileprotic; Gastrointestinal-Gen. - MECHANISM OF ACTION : Cell proliferation inhibitor. The ability of (I) to inhibit cell proliferation was tested using biological assays. The results showed that di(decanoyloxy)diphenylsi lane exhibited an IC50 value of 0.014 mM.
EP2379535A1 7-phenoxychroman carboxylic acid derivatives Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.
WO2005084786A1 Water containing oxygen nano bubbles and method for production thereof Oxygen nano bubbles capable of being present in an aqueous solution for a long period of time, which are produced by a method comprising applying a physical stimulus to oxygen-containing fine bubbles contained in an aqueous solution, to thereby reduce the bubble diameter of the fine bubble rapidly; and a method for producing such oxygen bubbles. Water containing the above oxygen nano bubbles is potentially useful in all technical fields, and in particular, the bioactive effect of such water on animals and plants has been found recently.
WO2006033007A3 Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one The present invention relates to novel polymorphic and amorphous forms of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one represented by formula (1), and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
CA2298522C 4-oxo-3,5-dihydro-4h-pyridazino[4,5-b]-indole-1-acetamide derivatives, their preparation and their application in therapy Compounds of general formula (I) (see formula I) in which X represents a hydrogen or halogen atom or a methyl, methoxy or phenylmethoxy group, Y represents a hydrogen atom, 1 or 2 halogen atoms or a hydroxyl, methoxy, nitro or methyl group, R1 represents a hydrogen atom or a (C1-C4) alkyl group, R2 and R3 each represent a hydrogen atom, a (C1-C4) alkyl group or a phenylmethyl group or else R2 and R3 form, with the nitrogen atom which carries them, an azetidinyl, pyrrolidinyl, 3--ethoxypyrrolidinyl, piperidinyl, morpholinyl, 4--methylpiperazinyl or 1,3-thiazolidinyl group. Application in therapeutics.
US20080031854 Thiolated macromolecules and methods of making and using thereof Described herein are thiolated macromolecules and methods of making and using thereof.
US20080161279 Methods of Treating Obesity The invention is directed to methods for treating and/or controlling obesity in a patient. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, AEGR-733 and implitapide) and a cholesterol absorption inhibitor (CAI) (for example, ezetimibe).
WO2009136214A1 Combination compositions comprising antimycotic agents and statins and the use thereof The present invention relates to a combination comprising one or more antimycotic agent(s) selected from the group of amphotericin B, nystatin, griseofulvin, primycin, terbinafine, an azole type one and one or more statin(s) selected from the group of lovastatin, simvastatin, fluvastatin, pravastatin, rozuvastatin, atorvastatin, cerivastatin, pitavastatin, for the use as an agent inhibiting the growth of fungi, furthermore, relates to a combination composition having antimycotic effect comprising a clinically acceptable dose of a combination of an antimycotic agent and a statin selected from the group of (i) amphotericin B and rozuvastatin, (ii) amphotericin B and pitavastatin, (iii) primycin and rozuvastatin, (iv) primycin and cerivastatin, (v) primycin and pitavastatin, (vi) voriconazole and simvastatin, (vii) voriconazole and pravastatin, (viii) voriconazole and atorvastatin, (ix) voriconazole and cerivastatin, and optionally one or more pharmaceutically acceptable excipients as well as relates to the said combination composition formulated as a medicine.˙
EP2776026A1 2-carboxamide cycloamino urea derivatives for use in treating vegf - dependent diseases The invention relates to the use of compounds of formula (I), in the treatment of warm-blooded animal target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical compositions comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.
US20090156680 Deodorants Containing Aminoacid Derivatives A deodorant composition comprising an aminoacid compound of formula I or II and a carrier material. I R1R2N—X—O—CH═CH—CH(NH2)CO2H II R1R2N—X—O—CH2CH2—CH(NH2)CO2H where X is an optionally substituted alkylene group comprising two carbons and R1 and R2 are independently H or CH3.
CN101386629B Water-soluble Pt(II) anticancer complexes using 3-acetoxy-1,1-cyclobutane dicarboxylic acid radical as leaving group The invention relates to a novel water-soluble platinum (II) anticancer complex, a leaving group of which is 3-acetoxy-1 and 1-cyclobutane dicarboxylate root (3-COO-CBDCA), and a carrier of which is an ammonia/amine ligand of a listed platinum antitumor drug. The carrier comprises ammonia (NH3), 1R, 2R-diamino cyclohexane (DACH), 1,2-bis (aminomethyl)-cyclobutane, 2-isopropyl-(4R, 5R)-4, 5-bis (aminomethyl)-1 and 3-dioxo-cyclopentane. The novel water-soluble platinum (II) anticancer complex can be synthesized by the normal preparation method of the platinum antitumor drug. The antitumor activity of the complex is equivlent to that of the prior carboplatin frequently used in clinic, and the toxicity and side-effect of the complex are obviously less than those of carboplatin, can be made into freeze-dried powder or injection for cancer treatment in clinic.
US20130281418 Use of hydroxypregnenolone derivatives for enhancing health and physical performance A method for the use of derivatives of hydroxypregnenolone (3-beta,17-alpha-dihydroxypregn-5-en-3-one) to enhance health and physical performance in humans and more particularly to the use of hydroxypregnenolone derivatives for restoring renal hormonal balance, decreasing body weight, reducing adipose tissue, increasing endurance, promoting skeletal muscle growth, boosting androgen levels, inhibiting aromatase, and increasing cognitive function.
WO2008065428A2 Steroid sulphatase inhibitors for treating hormone dependent cancer There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for the treatment of cancer, wherein the cancer is of a type in which the cancer cells overexpress aromatase enzyme.
US8058305 Pyrrolidine derivatives as prostaglandin modulators Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteoporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.
WO2008122618A1 Selective inhibitors of cb2 receptor expression and/or activity for the treatment of obesity and obesity-related disorders The invention relates to the use of a selective inhibitor of CB2 receptor expression and/or for the manufacture of a medicament indented for the treatment and/or the prevention of obesity and obesity-related disorders.
US20060003927 Modulation of immune function A method for modulating the immune system in a mammal is described comprising simultaneously, contemporaneously, separately or sequentially administering: i) an effective amount of an agonist of Notch signalling; and ii) an effective amount of an immunosuppressive agent.
US20110091449 Isolation of Anti-Desmoglein 1 Antibodies by Phage Display of Pemphigus Foliaceus Autoantibodies This invention relates to compositions and methods for the use of anti-autoimmune reagents that specifically bind to anti-desmoglein antibodies, which are responsible for pemphigus foliaceus. In addition, the invention relates to methods and compositions for inhibiting the expression or function of a variable region of an anti-desmoglein (anti-Dsg) pathogenic autoantibody.
US7485640 e.g. 2'-fluoro-5'-(7-methyl-8-oxo-7,8-dihydroimidazo[1,2-a]pyrazin-3-yl)-biphenyl-2-carbonitrile; anticonvulsant The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein —U—V— represents —CH═CH—, or —CH2—CH2—, —N═CH— or —CH═N—; X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— or —OCH2— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.
WO2014008503A1 Methods of using ceo2 and tio2 nanoparticles in modulation of the immune system Redox-active NPs are disclosed that can potentiate innate immunity and stimulate distinct adaptive responses, producing distinct T cell subset polarization outcomes. Nanomaterials that can alter the cellular redox environment through ROS modulation can impact human immunology. TiO2 nanoparticles potentiate DC maturation, inducing the secretion of IL-12, p70, and IL-1B, while treatment with CeO2 nanoparticles induces IL-10, a hallmark of suppression. When delivered to T cells, the materials direct distinct TH polarization, where TiO2 stimulates largely a TH1 dominated response, whereas CeO2 stimulates a TH2 bias and TReg differentiation.
CN102145035A Lotion for treating chilblain The invention provides a liquid medicine prepared by decocting a plurality of Chinese medical materials and adding yolk oil in a hereditary secret formula. For solving the technical problem, the invention adopts the scheme comprising the following steps of: putting a dosage containing five Chinese medical materials in different weights into a decocting pot once, wherein the five Chinese medical materials include 150g of safflower, 180g of narrowleaf spicebush branchlet leaf or root, 70g of fructus cnidii, 50g of radix sileris and 100g of tallow; adding water and decocting into a medicine; then, filtering, adding 50g of borneol and 50g of camphor and uniformly stirring; and finally, adding the yolk of a boiled egg in the hereditary secret formula; uniformly stirring into a lotion for treating chilblain. When the lotion for treating chilblain is in use, a person dips 10-50 ml of the lotion for treating chilblain and continuously rubs the chilblain part for 25-30 min. The invention has the advantages that the lotion for treating chilblain is easy to absorb by the epidermis of human bodies, and has short course of chilblain treatment, high curative effect and no recrudescence after healing.
WO2012130906A1 Derivatives useful for the treatment or prevention of bone tumors The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, where: X is a halogen atom or an OR3, SR3, or NR3R4 group; A1 is an X1-A3-X2 group in which X1 and X2 independently are an -O-, -S-, -NR5-, or -C=C- bond, and A3 is a (C1-C10)alkyl chain optionally interrupted by one or more unit, preferably one unit, selected from among -O-, -S-, -NR6-, -C(O)-, and -C=C-, or an optionally substituted aryl group; A2 is a -COOH-, C(O)O-((C1-C6)alkyl), or -C(OH)(PO3H2)2 group; and - R1 is a hydrogen atom or a -C(O)-((C1-C6)alkyl) group. The invention also relates to the use of said compound as a medicament, in particular for the treatment and prevention of bone tumors, pharmaceutical compositions containing the same, and a method for producing the same.
EP1443046B1 Novel 4-(2furoyl)aminopiperidines, intermediates in synthesizing the same, process for producing the same and medicinal use of the same Novel 4-(2-furoyl)aminopiperidines represented by the following general formula (I), intermediates in synthesizing the same, a process for producing the same and medicines containing the same as the active ingredient: (I) wherein X represents CH or N; and Y represents a group represented by the following general formula (II), (II-a) or (III): (II) (II-a) (III) (wherein a, b and c are each an integer of 0 to 6; Z represents CH2 or NH; W represents O or S; T represents O or N-R15 (wherein R15 represents H, C1-6 alkyl, benzyl or phenethyl); and R1 represents H, C1-6 alkoxycarbonyl, benzyloxycarbonyl, etc. Because of having an antagonism to opioid μ, these 4-(2-furoyl)aminopiperidine derivatives are useful in preventing or treating side effects of opioid μ receptor agonists selected from among constipation, nausea, vomiting and itch, constipation subitum, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic itch.
US20080090855 Substituted Cyclic Urea Derivatives and the Use Thereof as Vanilloid Receptor 1 Modulators The present invention relates to substituted cyclic urea derivatives corresponding to formula I, to processes for the preparation thereof, to medicinal drugs containing such compounds, to the use of such compounds in the preparation of medicinal drugs and in related treatment methods.
CN1634103A Clarithromycin orally disintegrating tablet Disclosed is a Clarithromycin oral disintegrating tablet and its preparation process, wherein the oral disintegrating tablet comprises clarithromycin and its medicinal salt of physiological effective dose and pharmaceutically acceptable carrying agent suitable for preparing orally disintegrating tablet, the pharmaceutically acceptable carrying agents suitable for preparing orally disintegrating tablet include macromolecular material, bulking agent, crumbling agent, effervescent agent, lubricating agent, flavoring agent and other pharmaceutically acceptable carrying agents suitable for preparing orally disintegrating tablet.
CN101269048A Lovastatin sustained-release dropping pill and preparation method thereof The invention discloses a drug compound for treating hyperlipemia and particularly relates to a prepared sustained-release lovastatin dropping pill adopting lovastatin as the ingredient. The drug compound aims to supplement the deficiency of the prior art and provide a sustained-release lovastatin dropping pill formulation. The sustained-release lovastatin dropping pill is prepared by adding stabilize Vitamin A and hydrophobic framework ingredients to the ingredients adopted by the prior art, thereby overcoming the defects in the prior art effectively, guaranteeing no occurrence of an obvious change related to the substance content for the drug during the effective storage period and having the advantages of full release, controllable release time, low frequency of drug taking and high bioavailability simultaneously. The sustained-release lovastatin dropping pill is suitable for clinical and family use.
WO2013090357A1 Hemostatic agents and methods of use Modified chitosan hemostatic agents include reverse micelles (10) having an outer hydrophobic shell (12) of suitable biocompatible hydrophobic components such as alkanes, and hydrophilic positively charged chitosan moieties (14) enclosed within the hydrophobic shell (12). The hydrophobic shell (12) may be formed by attaching hydrophobic moieties to one end of chitosan polymer molecules while retaining sufficient reactive (positively charged) amine groups on the remainder of the chitosan polymers for effective blood clotting. The resulting reverse micelles (10) have the capability of penetrating mucous membranes such as nasal mucosa (20) or otherwise penetrating to bleed sites shielded or partially shielded by mucosa or other tissues. Upon exposure to red blood cells (24) escaping from the bleed site (26) the positively charged interior of the reverse micelles breaks through the hydrophobic shell (12) to combine with the negatively charged red blood cells (24) thereby clotting and attenuating or stopping the bleeding.
WO2014078898A1 Chemotherapy for drug-resistant cancer cells The present invention relates to new treatments of multidrug resistant disorders, particularly cancers. There is provided a method of treating a cancer including administering an effective amount of a semicarbazone or hydrazone compound to a patient that has cancer, the cancer including a cancerous cell that includes an active efflux mechanism; wherein the compound is a substrate of the active efflux mechanism and the compound is able to form a chelation complex with a metal species in the cancerous cell, the chelation complex being cytotoxic to the cancerous cell.
US20090035368 Embedded micellar nanoparticles The present invention relates to a thermostable solid composition containing nanosized micelles, the micelles containing a poorly soluble chemical substance, such as a biologically active substance, dissolved in an auxiliary material, and the micelles being embedded in a water soluble carrier. The invention further relates to a process for preparing a thermostable solid composition and to a process for preparing pharmaceutical dosage forms comprising the same.
CN102321074A Indole ring-substituted pyrazole hydrazide derivative and preparation method and application thereof The invention relates to a series of indole ring-substituted pyrazole hydrazide derivatives and a preparation method and application thereof. The series of compounds have a structure shown as a general formula I; and as proved by an activity screening experiment, the compounds shown as the general formula I or salts thereof have cell proliferation inhibiting effects and can be taken as active ingredients for preparing medicaments for treating human body or animal solid carcinomas. The invention further relates to pharmaceutical application of a composition which contains the compounds shown as the general formula I. The general formula I is shown in the specifications.
CN1827109A Lyophilized injection powder using Lanluodier and its salt as active ingredients and preparing technique therefor This invention is about a freeze-dried preparation using Llandeilo and its salt as active components and its making method and usages. It is a medicine composition that takes Llandeilo and its salt as active components, and is formed by mixing acceptable finding. It can be used to emergency cure tachycardia arrhythmia (containing atria fibrillation, atria flutter and sinus tachycardia) during operation. It uses Llandeilo and its salt as raw materials, adds some findings of specify kinds and proportions, and develop freeze-dried preparation according to this invention for intravenous injection.
CN101390829A Anticancer composition loaded with anti-metabolism medicine fluorouracil and synergist thereof Disclosed is an anticancer, which contains antimetabolics fluorouracil and the synergist thereof, and is a sustained-release injection. The anti-cancer combination is composed of sustained-release microspheres and solvent; wherein, the sustained-release microsphere contains effective anticancer ingredients and auxiliary material; the solvent is common solvent or special solvent which contains suspending agent. The viscosity of the suspending agent is 100cp-3000cp (20 DEG C-30 DEG C) and is selected from carboxymethyl cellulose; the antimetabolics is selected from methotrexate, fluorouracil, carmofur, tegafur, decitabine, capecitabine or gemcitabine; the synergist is tetrazine medicine or anticancer antibiotics; the auxiliary material is selected from p(LAEG-EOP), p(DAPG-EOP), or polyphosphate copolymer, or copolymer or mixture of polyphosphate, polylactic acid, polifeprosan, sebacic acid and PLGA; the anticancer combination also can be made into sustained-release implants which can be injected or implanted in tumor or the periphery of tumor with the effective medicine concentration maintained for more than 50 days; meanwhile, the systemic reaction of the medicine is obviously reduced; the treatment effects of the non-operative treatments such as chemotherapy or radiation treatment are selectively enhanced.
CN101773498B Preparation method of oral slow/controlled-release preparation containing febuxostat The invention provides an oral slow/controlled-release preparation containing febuxostat and a preparation method thereof, which prepare the febuxostat into the long-acting oral slow/controlled-release preparation and can solve the problem that the incidence of an adverse reaction is increased because of the quicker dissolving-out and the burst effect of a common preparation existing in the priorart. The invention has the technical scheme that the oral slow/controlled-release preparation containing the febuxostat comprises the following components by weight percent: 5 to 60 percent of febuxostat, 10 to 50 percent of slow/controlled-release material, 20 to 80 percent of filling auxiliary material, 0.3 to 20 percent of adhesive and 0.1 to 7 percent of lubricant or glidant. Compared with a common quick-release preparation, the slow/controlled-release preparation can keep the effective and stable blood concentration for a longer time, avoids the burst effect of the quick-release preparation, lowers the incidence of the adverse reaction and enhances the application safety.
US20100183637 fusion molecule based on novel taa variant This invention provides novel carbonic anhydrase (CAIX) nucleic acid and peptide sequences, as well as related methods and compositions, including anti-cancer immunogenic agent(s) (e.g. vaccines and chimeric molecules) that elicit an immune response specifically directed against cancer cells expressing a CAIX antigenic marker. The novel CAIX variant and related compositions are useful in a wide variety of treatment modalities including, but not limited to protein vaccination, DNA vaccination, and adoptive immunotherapy.
WO2007135026A3 Substituted pteridines as therapeutic agents The invention relates to novel pteridines, suitable for the treatment of airway or gastrointestinal complaints or diseases, inflammatory diseases of the joints, the skin or eyes, diseases of the peripheral or central nervous systems, or cancerous diseases and pharmaceutical compositions comprising said compounds.
EP2522357A1 Treatment and/or prevention of inflammation and cutaneous photodamage and photoprotection of the skin with a water-soluble extract from plant of solanum genus The present invention relates to a pharmaceutical composition for preventing and treating inflammation and cutaneous photodamage, which contains a water-soluble extract from a plant of Solanum genus. The composition also has a photoprotective effect, and can be used as a cosmetic composition.
US20100249059 Bone filling complex and method for fabricating the same Provided is a bone filling complex and a method of preparing the same. The bone filling complex includes a matrix including a hydrogel-type hyaluronic acid derivative; and a bone derivative filling the matrix, and thus adhesion can be prevented and excellent bone generation property can be obtained. For example, the bone filling complex can be used to an injured portion of alveolar bone to derive an regeneration of the alveolar bone.
WO2012061057A1 Methods of treatment and/or prevention of scleroderma, uv injury or sunburn, formation of scars or keloids by using haloaryl substituted aminopurines Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.
EP2676960A1 Combination drugs comprising aminotetrahydropyrans as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes The present invention is directed to a combination comprising a compound of structural formula I or a pharmaceutically acceptable salt thereof and a biguanide; wherein the variables are as defined in the specification.Compouds (I) are inhibtors of the enzyme dipeptidyl peptidase IV (dpp4-inhibitors) and may be used in the reatment of diabetes.
CN101697972A Application of neoaspergillic acid in preparing antitumor drugs The invention belongs to the technical field of medicine and discloses an application of the neoaspergillic acid in preparing antitumor drugs. The neoaspergillic acid can be prepared by microbial fermentation or obtained by chemical synthesis. Tests prove that neoaspergillic acid has good suppressive activity to a plurality of cancer cells of people, and can be used for preparing antitumor drugs.
CN1626088A Hydrolase inhibitor of adenosine homeotypic cysteamine acid and usage An adenosine homotype of cysteine hydrolase depressant, 9-[(1'R, 2', S, 3'R)-2',3'-dihydroxycyclopentyl] adenine (DHCaA), 9-(trans-2', trans-3'-dihydroxycyclopentyl-4'-enylester) adenine (DHCeA) and its 3-site nitrogen analog is disclosed. It can be used to treat lupus erythematosus and allergic dermatitis.
CN102793715A Sargassum polysaccharide and application of Sargassum polysaccharide in medicine preparation used for treating kidney injury The invention relates to an application of Sargassum polysaccharide in medicine preparation used for treating kidney injury, the Sargassum polysaccharide is an active extract total polysaccharide in Sargassum graminifolium, the invention specifically relates to an application of Sargassum polysaccharide in kidney protection, and an application of Sargassum polysaccharide which can be mixed or individually used as antidotes in the pharmacy fields. The results show that the Sargassum graminifolium polysaccharide has certain protection effect on rat kidney, and can resist the kidney injury caused by medicines and chemicals such as gentamycin, cisplatin and high oxalic acid and the like.
US20080108681 Use of allantoin as a pro-collagen synthesis agent in cosmetic compositions Compositions comprising allantoin and an acceptable carrier and methods of using such compositions to increase pro-collagen synthesis in skin are disclosed. Compositions of the present invention may be used to decrease the signs of skin aging such as wrinkles and fine lines. Compositions of the present invention may be topically administered, orally administered or parenterally, such as administration by injection. When topically administered, additive ingredients such as penetration enhancers, fragrances, and moisturizers and cosmetic adjuvants may be included in compositions of the present invention.
CN103655469A Prescription and preparation technology of lipoic acid injection combination The invention discloses a prescription and a preparation technology of a lipoic acid injection combination. Each 1000 ml of injection comprises the components as follows: 25 g of lipoic acid, 5-8 g of a cosolvent ethanediamine and the balance of water for injection. The disclosed lipoic acid injection is stable in quality and resistant to hot pressure for sterilization, and the sterility level is high. The invention further provides the prescription and the preparation technology of the lipoic acid injection. The technology is simple, convenient and efficient, and the quality can be controlled.
CN1943639A An external use plaster for curing skin burn and scald The external use plaster for curing skin burn and scald is a kind of the Chinese medical preparation, mainly deal with the problem of scar coursed by skin burn and scald. Its character is: it is composed by the following ingredients of percent by weight: rhubarb(47-50), ossa draconis(20-25), borneol(8-12), catechu(40-60), sesame oil right volume, the application method is: use sesame oil to mix with the mixed powder of the left ingredients, so tomake them into cream. Apply the cream to the affected part, 1 time a day, 10 days as a period of treatmen. This invention has the effect of reducing fever, deintoxication, detumescence, antiphlogosis, promoting tissue and skin regeneration, promoting blood circulation, eliminating purulence, relieving pain. After the application, the burned and necrotic skin will be soon shed, and the burned or scald part will not scab.
EP1650210A1 Therapeutic agent for hyperpotassemia and bone disease The present invention has an object to provide a novel therapeutic agent for hypercalcemia and bone diseases, and a novel compound capable of being used as an active ingredient of the therapeutic agent. The present invention is a therapeutic agent for hypercalcemia or bone diseases, comprising as an active ingredient a reveromycin A derivative represented by the general formula (I) or a pharmaceutically acceptable salt thereof. (R represents a hydroxyl-protecting group releasable under acidic conditions.)
EP2641598A2 Orally administered pharmaceutical composition for the treatment of irritable bowel syndrome, comprising an intestinal motility modifier, an agent that prevents gas retention, and digestive enzymes, and preparation method thereof The invention relates to a pharmaceutical formulation or composition intended to be administered orally in the form of a tablet, a coated tablet or a capsule, for the prevention or treatment of intestinal disorders, such as irritable bowel syndrome, comprising an intestinal motility modifier, an agent that prevents gas retention, digestive enzymes, a binding agent, a diluent, an adsorbent agent, a disintegrating agent, a lubricant and a glidant, effective for normalising colon transit, for providing an analgesic activity, for providing an antispasmodic activity and for reducing symptoms related to intestinal gas, such as distention, abdominal pain and flatulence.
US20080188500 e.g. N-[4-methyl-3-(9H-pyrimido[4,5-b]indol-7-yl)phenyl]-3-(trifluoromethyl)benzamide; Janus kinases inhibitor; anticarcinogenic agent; immune-related diseases, skin disorders, myeloid proliferative disorders The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
CA2033640C Vaccines against cancer and infectious diseases A method of stimulating an immune response in a human against malignant cells or an infectious agent comprises the step of administering to the human an immunogenic amount of a primate anti-idiotype antibody or antibody fragment that acts as an immunogenic functional mimic of an antigen produced by or associated with a malignant cell or an infectious agent. Sub-human primate anti-idiotype antisera, especially from baboons, are preferred. Such anti-idiotype antibodies are used to make vaccines for inducing preventive immunity or a therapeutic immune response against tumors, viruses, bacteria, rickettsia, mycoplasma, protozoa, fungi and multicellular parasites.
CA2852274A1 Therapeutic combination for the treatment of cancer This invention relates to therapeutic combinations comprising a platinum-based antineoplastic agent, such as cisplatin, and an extract from a species of the genus Nerium, such as Nerium oleander, as well as methods of using such combinations to treat subjects, including humans, suffering from certain cancers, such as prostate cancer, melanoma, pancreatic cancer, lung cancer, breast cancer, or colorectal cancer.
CN103070888A Medicine for treating prosopoplegia A medicine for treating prosopoplegia belongs to the technical field of medicinal preparations. A technical scheme adopted by the invention is characterized in that each part of the medicine comprises 10-30mg of stiff silkworm, 10-30mg of scorpion, 10-30mg of lumbricus, 3-10mg of white sugar and 30-50mg of carp. The medicine has the efficacies of wind dispelling, spasm stopping, phlegm reducing, stagnation eliminating, endogenous wind calming, spasm calming, toxic substance counteracting, vein relaxing, pain relieving, heat clearing, convulsion arresting, panting calming, swelling reducing and qi descending.
EP2178873B1 6-phenyl-1h-imidazo[4,5-c]pyridine-4-carbonitrile derivatives as cathepsin inhibitors The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I), to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such asatherosclerosis,obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer,and chronic pain, such as neuropathic pain.
US7517683 Gene expression of alphavirus; nucleotide sequences; induce immunology response; aids vaccine Disclosed are alphavirus-based expression vectors expressing env, gag, pro, and/or pol genes of HIV-1, their transcripts, and transformed host cells. The present invention describes the expression of the Gag, Env, Pol, and/or Pro Proteins using the above expression vectors, and HIV-like particles (HIVLPs) composed of the above recombinant proteins. The virus-like particles (VLPs) of the present invention, as the mature and infective particles, are very useful as an antigen for a diagnostic kit for HIV infection as well as for a vaccine composition for prevention of HIV infection.
EP1716132A2 Spiro-benzodioxoles and their use as cb1 antagonists The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5 and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof, for use as therapeutically active substances. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB 1 receptors.
WO2012009262A3 Diclofenac salt of tramadol The present invention relates to a compound of diclofenac-tramadol salt in 1:1 ratio and a pharmaceutical formulation comprising such compound. The present invention also relates to a method for treating a patient with moderate to moderately severe pain. The method comprises: identifying a patient suffering from moderate to moderately severe pain with pain intensity scale of 5-9, and administering to said patient the diclofenac-tramadol salt, in an effective amount. The method is particularly useful in treating postoperative pain after Cesarean, postoperative pain after non-Cesarean surgeries, cancer pain, osteoarthritis pain, or rheumatoid arthritis pain.
EP2658535A1 Methods for facilitating muscle recovery after a period of disuse using beta-hydroxy-beta-methylbutyrate Disclosed are methods utilizing beta-hydroxy-beta-methylbutyrate (HMB) for facilitating the recovery of muscle after a period of muscle disuse. The HMB facilitates the recovery of muscle mass in an individual and can also be used to prevent further muscle atrophy typically associated with muscle reloading after extended periods of muscle disuse in the individual. The methods disclosed may be particularly suitable for older adults.
EP1687006B1 Pharmaceutical compositions for the treatment of renal dysfunction The present invention relates to a novel use of benzazepine-N-acetic acid derivatives which contain an oxo-group in the α-position to the nitrogen atom and are substituted in position 3 by a 1- (carboxyalkyl)cyclopentylcarbonylamino radical, and/or of their salts and biolabile esters, and/or of physiologically acceptable solvates thereof, in larger mammals and particularly in humans, preferably human patients having diabetes, and to the production of pharmaceutical compositions and products suitable for the novel treatment. The invention particularly relates to the treatment and/or prophylaxis of renal dysfunction, disease or disorder, preferably in diabetic patients, but in a broader sense also in patients with syndrome X or in particular in patients with a renal dysfunction, disease and /or disorder, which patients are in addition hypertensive, obese, hyperglycemic and/or subject to metabolic disorder.
WO2012135736A2 Modulation of signal transducer and activator of transcription 3 (stat3) expression Disclosed herein are antisense compounds and methods for decreasing STAT3 mRNA and protein expression. Such methods, compounds, and compositions are useful to treat, prevent, or ameliorate hyperproliferative diseases.
US20080234347 Administering a hexahydrocycloheptapyrazole derivative, e.g., 8-(3-chloro-benzyl)-1,4,5,6,7,8-hexahydro-cycloheptapyrazole-3-carboxylic acid [(1S)-2-hydroxy-1-phenyl-ethyl]-amide; treating various kinds of pain including postoperative, inflammatory or neuropathic or the result of injury or age The present invention is directed to a method for treating, ameliorating or preventing CB2 receptor mediated pain in a subject in need thereof comprising administering to the subject an effective amount of a compound of formula (I): or a form thereof, wherein X1R1, X2R2, X3R3, X4R4 and X5R5 are as defined herein.
WO2012167081A1 Hydrazino 1h-imidazoquinolin-4-amines and conjugates made therefrom 1H-Imidazo[4,5-c]quinolin-4-amines substituted at the 1-position with a substituent bearing a hydrazinobenzamide or hydrazinonicotinamide, a salt thereof, or a protected hydrazinobenzamide or hydrazinonicotinamide and conjugates made from such compounds are disclosed. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed.
CN103230379A Orally disintegrating sustained-release preparation containing tamsulosin hydrochloride and preparation method thereof Belonging to the field of medicines, the invention particularly relates to a preparation method of a sustained release tablet containing tamsulosin hydrochloride. The dosage form is an oral preparation that is prepared by taking tamsulosin hydrochloride as an active component and using acceptable auxiliary materials in an orally disintegrating tablet. The preparation not only has the characteristics of rapid disintegrating speed, rapid onset, and high patient compliance of orally disintegrating tablets, but also has the advantages of long action time, significantly reduced adverse reactions during instantaneous release of drugs, and stable blood concentration.
US20080213216 Transgenic lymphocytes comprising expression vector coding Fc receptor for use in identifying modulators for prevention and treatment of ifection and immune system disorders The present invention relates, in general, to methods of stimulating phagocytosis and thereby combating infection and/or modulating immune complex disease, in particular, to methods of modulating the number and type of Fc receptors present on cells that normally possess such receptors, including monocytes and macrophages, as well as on cells that normally do not possess Fc receptors, such as fibroblasts, and to compounds and compositions suitable for use in such methods.
US7700632 3-(3-Chloro-biphenyl-4-yloxymethyl)-benzoic acid; antidiabetic; type 2 diabetes, insulin resistance, impaired glucose tolerance, obesity The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.
CN101953812A Lansoprazole enteric coated tablet and preparation method thereof The invention relates to the field of medical preparations, in particular to a Lansoprazole enteric coated tablet and a preparation method thereof. The Lansoprazole enteric coated tablet of the invention comprises the following components from inside to outside: a. a tablet core composed of Lansoprazole and pharmaceutical excipients; b. an intermediate isolated layer composed of opacifier and lubricating agent; and c, an enteric coated layer composed of methacrylic acid copolymer and medicinally pharmaceutical excipients. The Lansoprazole enteric coated tablet is characterized in that the tablet core is prepared by the following steps: granulating the Lansoprazole, diluent, solubilizer, alkaline stabilizing agent and disintegrating agent; adding disintegrating agent again; and pressing. The Lansoprazole enteric coated tablet of the invention has the advantages of simple preparation process, low equipment requirement, large production quantity, controllable product quality, rapid medicine dissolution rate, good repeatability and stability, and suitability for industrial large-scale product.
CN101843623A External fat-increasing preparation and application thereof The invention provides an external fat-increasing preparation. Active ingredients contained in the external fat-increasing preparation are oleanolic acid and/or a material which can provide the source of the oleanolic acid for a body. In addition, the invention also provides the application of the oleanolic acid and/or the material which can provide the source of the oleanolic acid for the body in the preparation of the external fat-increasing preparation. The external preparation for increasing fat for human beings or mammals is prepared by using the oleanolic acid and/or the material which can provide the source of the oleanolic acid for the body as an active ingredient for generating a fat-increasing effect, so that an unforeseeable technical effect is generated. Animal experiments and clinical verification show that the external preparation can transfer medicaments from the surface layer of skin to the deep layer of the skin and/or a circulatory system, so that fat issues are effectively increased or thickened and beautifying and/or medical effects are generated on the human beings or the mammals.
CN102078598A Injection for preventing and treating porcine viral diseases and preparation method thereof The invention belongs to the technical field of veterinary medicine, specifically to an injection for preventing and treating porcine viral diseases and a preparation method thereof. Every 1000ml of the injection contains 1 to 100g of thymopoietin, 1 to 10*10 <8> IU of interferon, 10 to 50 million units of gentamycin sulfate, 0.1 to 2g of antioxidant, 0.2 to 0.4g of protective agent, 50 to 100ml of buffer, 20 to 80ml of osmotic pressure adjusting agent, a pH adjusting agent and the balance of water for injection. The preparation in the invention is wide in application, fast in curative effect, little in medicine dosage, low in cost, and difficult to bring germ contamination. The injection reduces the stress reaction caused by capturing the animal for many times in injecting, and overcomes the shortcoming that the water needle made of thymopoietin and interferon is unstable.
WO2012058211A3 Quinazoline derivatives, compositions, and uses related thereto The invention relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the invention relates to inhibitors of NADPH-oxidase.
US20110015167 Use of norgestimate as a selective inhibitor of trpc3, trpc6 and trpc7 ion channels TRPC ion channels are non-selective channels widely expressed in human tissues. These channels are involved in numerous physiological functions and are putative targets for the development of novel medicines. There is a need to gain a better understanding of TRPC ion channels in cells and beyond. The present invention provides a pharmacological tool compound that allows to study TRPC ion channels due to its discriminating inhibition of TRPC subfamilies. In the present invention, norgestimate is shown to selectively inhibit TRPC3, TRPC6 and TRPC7.
WO2011079507A1 Use of pacitaxel and docetaxel The present invention discloses the use of paclitaxel as adjuvant of vaccines, and further discloses the use of docetaxel as adjuvant of vaccines. The vaccines are protein vaccine, nucleic acid vaccine, polypeptide vaccine or whole virus vaccine. Paclitaxel and docetaxel can improve the response intensity of cellular immunity and humoral immunity induced by vaccines, reduce the stimulus response of injection site, and prolong the storage period of vaccines.
CN103212087A Antibiotic-chitosan covalent conjugate and preparation method and application thereof in preparation of anti-tumor medicines The invention discloses an antibiotic-chitosan covalent conjugate and a preparation method and application thereof in preparation of anti-tumor medicines. The preparation method comprises the following steps of: (1) preparing a chitosan water solution and an antibiotic water solution, mixing in a mole ratio of chitosan to antibiotic being 1:0.5-1:10, adding NaCNBH3, stirring by shielding sunlight, and reacting for 15-72 hours at 15-30 DEG C; (2) transferring the water solution obtained by the step (1) to a dialysis bag with molecular cut off of 1400-10000, and performing dialysis for 1-5 days to obtain a dialysis liquid; and (3) drying the dialysis liquid obtained by the step (2). The obtained antibiotic-chitosan covalent conjugate has stronger damaging effect to tumor cells, treats tumors in wide range, and is exact in effective components.
CN101278919B Metformin hydrochloride and Glipizide sustained-release pellet and method of preparing the same The invention discloses a metformin hydrochloride and glipizide sustained-release pellet and a preparation method thereof. In the preparation method, a sustained release coated pellet of the metformin hydrochloride and a sustained release pellet of the glipizide are prepared respectively; and the two pellets are filled in capsules in a proportion of 250g-500g of the metformin hydrochloride and 2.5g-10g of the glipizide in every 1000 capsules; wherein, the coated pellet of the metformin hydrochloride is prepared by pill pericardium sustained release coating membrane; the sustained release pellet of the glipizide is prepared directly by extrusion-spheronization method. In the invention, the two pellets are filled into one capsule, thereby being convenient for quality control; octodecyl alcohol is taken as sustained release material for the sustained-release pellet of the glipizide, which is convenient for the forming of the pellet so as to reduce bursting release effectively. The metformin hydrochloride and the glipizide slowly release a drug within 12 hours, which reduces the frequency of taking medicine, stabilizes blood concentration better and reduces untoward effect, thereby having good marketing prospect.
US20050009144 Transgenic cell comprising nucleotide sequences coding endostatins for use as tool in identifying modulators for treatment and prevention of cell proliferative and angiogenesis-related disorders The present invention relates to polynucleotides associated with angiogenesis-related disorders. The present invention also relates to canine endostatin genes, novel genes associated with angiogenesis-related disorders, such as cancer. The invention encompasses endostatin nucleic acids, recombinant DNA molecules, cloned genes or degenerate variants thereof, endostatin gene products and antibodies directed against such gene products, cloning vectors containing mammalian endostatin gene molecules, and hosts that have been genetically engineered to express such molecules. The invention further relates to methods for the identification of compounds that modulate the expression of endostatin genes and gene products and to using such compounds as therapeutic agents in the treatment of angiogenesis-related disorders, e.g., cancer. The invention also relates to methods for the diagnostic evaluation, genetic testing and prognosis of angiogenesis-related disorders, e.g., cancer, and to methods and compositions for the treatment these disorders.
WO2013127913A1 4,4-difluoro-piperidine-compounds The invention, in a first aspect relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 6-membered aromatic ring, or a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, or a 6-membered benzocondensed heteroaromatic ring containing N as heteroatom, optionally each of said rings being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, cyano, trifluoromethyl, dimethylamino, or phenyl which optionally is substituted with one or more halogen atoms, or a 5- or 6-membered heterocycle containing from one to three nitrogen atoms; X is O or N; P is pyridyl, pyrimidyl, pyrazyl, or pyridazyl, each being optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, and cyano, and use thereof as pharmaceuticals.
CN102451165A Rotundine orally disintegrating tablets and preparation method thereof The invention relates to rotundine orally disintegrating tablets and a prescription and process for preparing the rotundine orally disintegrating tablets by adopting a freeze drying method. The rotundine orally disintegrating tablets are prepared from rotundine as a main medicine and pharmaceutic adjuvants, can be taken without water, are capable of rapidly disintegrating after entering the mouth, are suitable for taking by patients suffered from dysphagia, such as the old, children and the like, are simultaneously suitable for medications in the travel journey under the condition of being not easy to obtain a water source, has the advantages of convenience for taking, high absorption speed, small fast pass effect, little irritation to digestive tract mucosa, wide market application prospect and the like, and are capable of remarkably reducing side effects of rotundine. In addition, the invention also relates to a preparation method of the rotundine orally disintegrating tablets.
EP1701726A4 Antimicrobial photodynamic therapy compound and method of use A method and composition for destroying microbes, especially bacteria, in the body utilizing Safranin O in conjunction with electromagnetic radiation is disclosed. In a preferred method, a composition comprising Safranin O is introduced to a treatment area. After a sufficient period of time has elapsed, radiation of a suitable wavelength is applied to the area to activate the Safranin O and by a photodynamic reaction to destroy the bacteria. Preferred radiation has a wavelength around 530 nm. This method is effective for destroying both Gram-positive and Gram-negative bacteria, and is particularly effective in areas where complex media such as blood serum, blood or saliva are also present.
EP1565475B1 Diazinopyrimidines and their use as protein kinase inhibitors The present invention provides a compound of the formula: (I) ;or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X1, X2, and Ar1 are as defined herein. The present invention also provides a process for producing the same, compositions comprising the same, and methods for using the same.
WO2014108570A1 GALACTOSAMINOGALACTAN COMPRISING α1-4 LINKED GALACTOSE AND α1-4 LINKED N-ACETYLGALACTOSAMINE FOR USE IN THE TREATMENT OF AT LEAST ONE INFLAMMATORY DISEASE A first object of the invention is galactosaminogalactan comprising α1-4 linked galactose, α1-4 linked N-acetylgalactosamine, and optionally α1-4 linked galactosamine, for use in the treatment of at least one inflammatory disease. Another object of the invention is a pharmaceutical composition comprising a galactosaminogalactan comprising α1-4 linked galactose, α1-4 linked N-acetylgalactosamine, and optionally α1-4 linked galactosamine, as defined herein, and optionally a pharmaceutically acceptable carrier. Another object of the invention is a pharmaceutical composition according to the invention, for use in the treatment of at least one inflammatory disease. Another object of the invention is an inhibitor of IL-1RA for use in the treatment of human fungal diseases. Another object of the invention is a pharmaceutical composition comprising an inhibitor of IL-1RA, and optionally a pharmaceutically acceptable carrier.
EP1032696B1 Vector for tissue-specific replication and gene expression The invention generally relates to cell-specific expression vectors. It particularly relates to targeted gene therapy using recombinant expression vectors and particularly adenovirus vectors. The invention specifically relates to replication-conditional expression vectors and methods for using them. Such vectors are able to selectively replicate in a target cell or tissue to provide a therapeutic benefit in a tissue from the presence of the vector per se or from one or more heterologous gene products expressed from the vector and distributed throughout the tissue.
US20060079458 Using heat shock proteins to improve the therapeutic benefit of a non-vaccine treatment modality The present invention relates to methods of improving a treatment outcome comprising administering a heat shock protein (HSP) preparation or an α-2-macroglobulin (α2M) preparation with a non-vaccine treatment modality. In particular, an HSP preparation or an α2M preparation is administered in conjunction with a non-vaccine treatment modality for the treatment of cancer or infectious diseases. In the practice of the invention, a preparation comprising HSPs such as but not limited to, hsp70, hsp90 and gp96 alone or in combination with each other, noncovalently or covalently bound to antigenic molecules or α2M, noncovalently or covalently bound to antigenic molecules is administered in conjunction with a non-vaccine treatment modality.
US20050119343 Crystalline form; inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase; for oral administration The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a crystalline hydrated form of the calcium salt of dihydroxy open acid simvastatin to a patient in need of such treatment. Methods for making the calcium salt of dihydroxy open acid simvastatin are also provided.
WO2005032580A1 Methods and compositions for treating eosinophil mediated gastro-intestinal dysfunction or disease The present invention provides methods and compositions for the effective treatment of gastro-intestinal dysfunction, including chronic and acute inflammatory bowel diseases and the symptoms thereof, through the modulation of eosinophil peroxidase activity. The methods and compositions disclosed include those that modulate eosinophil peroxidase activity by depleting substrate, antagonizing enzyme activity, or attenuating enzyme expression so as to effect treatment of disease conditions or symptoms. Also provided are methods for the identification of additional therapeutically effective compounds for the treatment of gastro-intestinal dysfunction through the modulation of eosinophil peroxidase activity.
CN102048716A New application of hydroquinone compound The invention relates to new application of a hydroquinone compound, particularly application of a hydroquinone compound (shikonin) in preparing medicines for resisting hepatitis C virus (HCV). The hydroquinone compound (shikonin) has obvious activity for resisting HCV, and the selection index is up to 43.56; and thus, the hydroquinone compound (shikonin) can be used as a lead compound for treating hepatitis C. The molecular formula of the hydroquinone compound (shikonin) is C16H16O5, and the chemical structural formula is disclosed in the specification.
CN101384254A Use of a compound that enhances gabaa-ergic neurotransmission for the treatment of inflammatory diseases The present invention relates to the use of gaboxadol, or a combination of gaboxadol and one or more anti-inflammatory compounds, for the treatment of an inflammatory disease. The present invention further relates to a pharmaceutical composition comprising gaboxadol and one or more anti-inflammatory compounds. The present invention further relates to a method of treating a 5 disease wherein one or more inflammatory markers are increased, comprising administering to a subject in need thereof a therapeutically effective amount of a compound that enhances GABAA- ergic neurotransmission.
CA2611655A1 Skin-piercing device for treatment of acne The invention features a skin-piercing device having a piercing element and the use thereof of treating acne.
US7452894 Purine derivatives as purinergic receptor antagonists Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; R3 is selected from H, alkyl, COR8, CONR9R10, CONR8NR9R10, CO2R11 and SO2R11; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an (NR5R6) group then R5 and R6 may be linked to form a heterocyclic ring; R7 is selected from alkyl and aryl; R8, R9 and R10 are independently selected from H, alkyl and aryl, or R9 and R10 may be linked to form a heterocyclic ring, or where R8, R9 and R10 are in a (CONR8NR9R10) group, R8 and R9 may be linked to form a heterocyclic group; and R11, is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or for neuroprotection in a subject; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se.
CN1615832A Ritodrine hydrochloride powder injection and preparing method Ritodrine hydrochloride as main medicinal component or Ritodrine hydrochloride as main medicinal component and with at least one of dextran, mannitol and sorbic alcohol added as medicine stuffing is dissolved in at least one kind of solvent selected from injection water, acetone and alcohol to prepare solution; and the solution is decolored with active carbon, filtered with microporous film and freeze dried or decompression dried to obtain the powder for injection. The present invention has the features of advance preparation process, high product stability, convenient transportation, and convenient and effective product. The medicine of the present invention is used clinically in inhibiting contraction of uterine smooth muscle, reducing uterine activity to prolong the gestational period, preventing abortion caused by gynecologic treatment, etc.
WO2013095027A1 Anti-inflammation composition using vladinol f The present invention relates to an anti-inflammation composition using Vladinol F which is an active material isolated from Ficus erecta var. sieboldii (Miq.) King. Vladinol F, which is an active material, has an activity of inhibiting the generation of NO, an activity of inhibiting the generation of PGE2, and an activity of inhibiting the generation of inflammatory cytokines (TNF-α, IL-1β and IL-6), INOS and COX-2.
WO2011147964A1 Formulation containing azelaic acid and having a pigment addition The present patent application relates to a pharmaceutical composition containing azelaic acid, preferably a gel containing azelaic acid and having a pigment addition, which can be used, amongst others, for treating rosacea and acne, and to a method for producing same.
US20100285119 Multiparticulate Extended Release Pharmaceutical Composition Of Carbamazepine And Process For Manufacturing The Same Disclosed herein is an extended release pharmaceutical composition comprising at least two populations of extended release minitablets having a core comprising carbamazepine or its pharmaceutical salts, solvates, hydrates, an extended release polymer(s), wherein the extended release polymer of each population of minitablets is unalike. The process for manufacturing said composition is also disclosed.
WO2013170719A1 Vinorelbine derivatives, pharmaceutical composition, preparation method therefor and application thereof Disclosed are vinorelbine derivatives represented by formula (I), or pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising a therapeutically effective amount of vinorelbine derivatives or pharmaceutically acceptable salts thereof. Also disclosed are preparation method of vinorelbine derivatives or pharmaceutically acceptable salts thereof, and application in the preparation of medicaments for treating tumors. The vinorelbine derivatives show inhibiting activities against several human tumor cell lines and can be used as medicaments to treat malignant tumors.
US20070105850 2,4-diChloro-N-(4-cyclopropylmethanesulfonyl-1-cyclopropylmethylcyclohexyl-methyl) benzamide; glutamatergic neurotransmission dysfunction and diseases; dementia; antidepressants; learning enhancement; cognition activators; attention deficit disorders; autism; eating disorders; anxiolytic agents Compounds of formula (I) or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
WO2006015775A2 Egfr kinase inhibitor combinations for treating respiratory and gastrointestinal disorders The present invention relates to novel pharmaceutical compositions comprising at least one EGFR kinase inhibitor and at least one additional active compound selected from beta-2 mimetics, steroids, PDE-IV inhibitors, p38 MAP kinase inhibitors, NK1 antagonists and endothelin-antagonists, processes for preparing the compositions and the use thereof as medicament in the treatment of respiratory or gastrointestinal complaints, as well as inflammatory diseases of the joints, the skin or the eyes.
CN101375860B Application of cisplatin combined with hTERT-HRP/IAA in medicament for treating cervical cancer The invention discloses an application of cisplatin combined with phTERTp-HRP/IAA in drugs for the treatment of cervical cancer cells, in particular to the strengthening role of the cisplatin on the activity of a hTERT gene promoter. The cisplatin and the phTERTp-HRP/IAA are commonly used in the synergy for killing the human cervical cancer cells, and the action mechanism thereof is further explored. The application adopts Hela cells for carrying out the study and evaluates the impacts of the cisplatin on the activity of the hTERT promoter through the expression of downstream luciferase reporter gene regulated by the hTERT promoter. The synergic killing role and the mechanism of the cisplatin and the hTERT promoter during the combined use for regulating the gene therapy of an HRP/IAA system are evaluated through the detection of cell proliferation rate, cell apoptosis rate and cell cycle. The results confirm that the cisplatin can strengthen the activity of the hTERT gene promoter; and when in combined use with the phTERTp-HRP/IAA, the killing role of the human cervical cancer cells is significant.
CN103142471A Calcitriol solution and preparation method thereof The invention relates to a calcitriol solution and a preparation method thereof. The solution is prepared from the following ingredients in percentage by weight: 0.0005% of calcitriol, 0.9-1.2% of meglumine, 27-30% of polyethylene glycol 400, 12-14% of polyethylene glycol 6000, 0.2% of antioxidant, 0.5% of flavoring agent and the balance of distilled water. Compared with the prior art, the solution has the advantages that the content of calcitriol is remarkably increased, so that the drug dosage is reduced; and the stability of calcitriol to light and air is improved, and the bioavailability of calcitriol is also remarkably improved.
CN102846501A Application of ginkgolic acid in skin whitening, freckle removing and resurfacing The invention relates to application of ginkgolic acid in skin whitening, freckle removing and resurfacing. The ginkgolic acid comprises ginkgolic acid, ginkgol and bilobol and can be obtained from the extracts of such parts of the gingko as leaves, fruits, testae and rootstalks by a chemical separation method. A medicament or cosmetic which contains ginkgolic acid and is used for skin whitening, freckle removing and resurfacing contains 0.001-80% by weight of ginkgolic acid and pharmaceutically common external preparation substrates or acceptable carriers, wherein the preparation is any one pharmaceutically called external dosage form. Pharmacological experiment studies show that the preparation has the effect of inhibiting the activity of tyrosinase and melanogenesis in the skin, can obviously promote proliferation of keratinocytes and apoptosis and has obvious skin whitening, freckle removing and resurfacing effects. Clinical trials show that the preparation has obvious effects of improving the preventing dark yellow complexion and facial pigmentation, is one hundred percent in effective rate, is safe to use and does not have side effects.
CN1853631A Fast disintegrant containing paroxetine A fast disintegrating tablet contains the paroxetine particles coated by acrylic resin, hydroxypropyl methylcellulose, or their mixture, excipient and disintegrant. Its disintegrating speed in saliva is shorter than 30 s.
WO2009002534A1 Imidazopyridinyl thiazolyl histone deacetylase inhibitors A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
WO2010001365A1 Nitrogen heterocycle derivatives as proteasome modulators The instant invention relates to the use of at least one nitrogen heterocycle derivative of formula (I): as proteasome activity modulator in the manufacture of a pharmaceutical composition intended to prevent and/or treat a disease condition mediated by the proteasome activity.
US20120039823 Preparations for reducing itching and other paraesthesias with (1r,2s,5r)-2-isopropyl-5-methyl-n-(2-(pyridin-2-yl)ethylcyclohexanecarboxamide and/or (1r,2s,5r)-n-(4-(cyanomethyl)-phenyl)-2-isopropyl-5-methylcyclohexanecarboxamide and/or (1r,2s,5r)-n-(4-(cyanomethyl)-phenyl)-2isopropyl-5-methylcyclohexanecarboxamide Use of topical, cosmetic or dermatological preparations with a content of (1R,2S,5R)-2-isopropyl-5-methyl-N-(2-(pyridin-2-yl)ethylcyclohexanecarboxamide and/or (1R,2S,5R)-N-(4-(cyanomethyl)-phenyl)-2-isopropyl-5-methylcyclohexyl carboxamide for reducing itching.
CN103735846A Chilblain cream and preparation method thereof The invention discloses chilblain cream and a preparation method thereof. The chilblain cream is prepared from the following components in parts by weight: 25-45 parts of Chinese angelica, 15-25 parts of safflower, 20-30 parts of dahurian angelica, 25-35 parts of cinnamon, 10-20 parts of bletilla, 20-30 parts of aloe gel juice, 5-10 parts of beewax tea-seed oil, 20-30 parts of snake oil, 10-20 parts of vitamin B3, and 15-30 parts of allantoin. The chilblain cream has the beneficial effects of small toxic or side effect, high wound healing speed, good itching relieving effect, excellent treatment effect and low price.
US7148220 Tyrosine kinase enzyme inhibitors as growth factor receptors and useful as antiproliferation agents The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
US8198282 Substituted azaquinazolines having an antiviral action This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.
US20110165277 Biological Materials and Uses Thereof There is provided the use of a sandalwood extract or a sandalwood analogue as an additive to animal foodstuff for the reduction of methane production, reduction of bacterial mediated protein breakdown and reduces bacterial growth in the stomach. There are also provided food products and methods of making food products incorporating sandalwood extracts or sandalwood analogues.
US20110263677 Gos2 modulators in the treatment of acne, of seborrhoeic dermatitis or of hyperseborrhoea An in vitro or in vivo method for screening for candidate compounds for the preventive or curative treatment of acne, of seborrhoeic dermatitis or of skin disorders associated with hyperseborrhoea, includes determining the ability of a compound to modulate the expression or the activity of G0/G1 switch protein 2 (GOS2), and also utilizes modulators of the expression or of the activity of this protein, for the treatment of acne, of seborrhoeic dermatitis or of skin disorders associated with hyperseborrhoea; methods for the in vitro diagnosis of or in vitro prognosis for these pathologies are also featured.
CN101229217A Channels and collaterals uncloging acupuncture medicine The invention discloses a medicine for dredging meridian and moxibustion therapy; the invention comprises the following medical materials: moxa of 3 to 5g, borneol of 1 to 3g, catechu of 3 to 5g, and pearl powder of 2 to 3g. The invention has the efficacy of dredging meridian, replenishing Qi and blood, regulating Yin and Yang, and anti-aging. Through dredging meridian, the invention can stop pain, be detumescent, strengthen the tensile force of muscle and restore the muscle function, and accelerate blood circulation and nerve conduction, and the invention can also treat cervical spondylosis, lumbar vertebrae disease, disc herniation and expansion, stenosis of verterbral tube, stroke and sequelae, face paralysis and strong sequelae, amyotrophy, twig neuritis, and damage of nerve cell. By adopting the method of treating internal diseases through external methods, the invention belongs to physiotherapy, and is characterized by being rapidly absorbed by the skin and no toxic and side effect.
EP2604262A1 Composition comprising a reduced isoalpha acid, a mineral and a vitamin for use in the treatment of autoimmune diseases The present invention relates to the use of a composition comprising a synergistic combination of (a) at least one reduced isoalpha acid compound selected from the group consisting of dihydro-isohumulone, dihydro-isocohumulone, dihydro-isoadhumulone, tetrahydro-isohumulone, tetrahydro-isocohumulone, tetrahydro-isoadhumulone, hexahydro-isohumulone, hexahydro-isocohumulone, and hexahydro-isoadhumulone, (b) at least one mineral, and (c) at least one vitamin for the manufacture of a medicament for the treatment of an autoimmune disease in a mammal; wherein the combination of (a), (b) and (c) provides a combination index (CI) of less than 1 for synergistic inhibition of PGE2 production.
CN102000031A Method for preparing fluorocarbon microspheres The invention relates to a method for processing fluorocarbon microspheres, which comprises the specific steps of: dissolving fluorocarbon and a fluorine-containing surfactant in water to form an internal water phase; with an organic solution containing a surfactant and a shell material as an oil phase and a water solution containing a dispersing phase as an external water phase, after uniformly mixing the internal water phase, the oil phase and the external water phase according to the volume ratio of 1:3:20-1:10:100, fully stirring to prepare a micro emulsion, and evaporating solvent; and then washing with distilled water, and eccentrically separating to obtain the fluorocarbon microspheres. The fluorocarbon microspheres prepared by the method have entrapment rate of 60-80 percent and diameter of 500nm-2mum, and are suitable for long-term storage. The method has the advantages of simple process, convenience for operation, remarkable emulsifying effect, better stability of the emulsion, and capability of continuous production.
CN103705473A Lansoprazole freeze-dried powder injection and preparation method thereof The invention discloses lansoprazole freeze-dried powder injection which does not contain mannitol. The freeze-dried powder is pre-frozen in a gradually cooling mode, so that lansoprazole, sodium hydroxide and meglumine are eutectic in the pre-freezing process, the freeze-dried powder is redissolved by adding water, the dissolution speed is high, and visible foreign matters and insoluble particles are good.
US20100048524 Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.
CN102895656A Adenosine triphosphate-coenzyme-insulin compound-containing pharmaceutical composition The invention provides an adenosine triphosphate-coenzyme-insulin compound-containing pharmaceutical composition, which comprises the following components: 15-25mg of adenosine triphosphate, 40-60 units of coenzyme A, 3-5 units of insulin, 4-8mg of arginine, 3-7mg of low molecular dextran, and 2-4mg of NaOH. For solutions of different properties, different dissolution strategies are adopted in a preparation process, thus maintaining the efficacy of various drugs as much as possible. By rational allocation of various components of the pharmaceutical composition, the dosages of auxiliary materials are reduced, so that the pharmaceutical composition provided in the invention not only has reduced cost, but also has increased stability and medication safety.
CN103709115A Pleuromutilin antibiotic derivatives The present invention relates to pleuromutilin antibiotic derivatives represented by a general formula (I), pharmaceutically acceptable salts, prodrugs, solvates or stereoisomers thereof, wherein R<2>, Q<1>, Q<2>, m and X are defined in an instruction. The present invention further relates to preparation methods of the compounds, drug compositions containing the compounds, drug preparations containing the compounds, and applications of the compounds in preparation of drugs for treatment and/or prevention of diseases caused by microorganisms.
CA2844930A1 Compositions and methods for inducing apoptosis Methods and compositions are provided for generating novel nucleic acid molecules through targeted spliceosome mediated RNA trans-splicing (SMaRTTM) that result in expression of a splicing isoform or variant thereof. The methods and compositions are based upon pre-trans-splicing molecules (PTMs) designed to interact with a target pre-mRNA molecule and mediate a trans-splicing reaction generating a novel chimeric RNA molecule encoding a splicing isoform for the treatment of a variety of gene isoform induced diseases such as cancer.
WO2014028756A1 Deuterated baricitinib The present invention in one embodiment provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification.
US20090312283 Branched hyaluronic acid and method of manufacture A branched hyaluronic acid, wherein the linear backbone comprises hyaluronic acid in which one or more N-Acetyl-Glucosamine has been deacetylated to Glucosamine, with branching sidechain(s) covalently linked to the primary amine(s) of said deacetylated Glucosamine thus forming a secondary amine(s); a precursor for producing said branched hyaluronic acid; and a method for producing said branching hyaluronic acid
US20050159481 4,6-di-t-butyl-5-hydroxy-2,2-di-n-pentyl-2,3-dihydrobenzofuran; side effect reduction: lowers high-density lipoprotein cholesterol (HDL-C), prolongs electrocardiographic QT intervals; myocardial infarction, hypotensive, antidiabetic, anticoagulant, arteriosclerosis obliterans, intermittent claudication Herein provided is a novel pharmaceutical composition for ameliorating the vascular tone-regulating function of vascular endothelium, comprising a compound represented by formula (1): wherein R1 represents a hydrogen atom or an acyl or arylalkyloxycarbonyl group; R2 and R3 are identical or different and represent an optionally substituted alkyl group, an optionally substituted alkenyl group or an optionally substituted alkynyl group; or R2 and R3 may together form a cycloalkyl group.
CN101954067A Aqueous solution of recombinant human serum albumin-interferon alpha fusion protein and preparation method thereof The invention relates to stable aqueous solution of a recombinant human serum albumin-interferon alpha fusion protein and belongs to the technical field of biological preparations. The aqueous solution of the recombinant human serum albumin-interferon alpha fusion protein is prepared by dissolving the recombinant human serum albumin-interferon alpha fusion protein and pharmaceutically acceptable stable auxiliary material in pharmaceutically acceptable buffer solution, and is characterized in that the pharmaceutically acceptable stable auxiliary material is arginine at a concentration of 5 to 30 g/L. The aqueous solution of therecombinant human serum albumin-interferon alpha fusion protein can prevent the aggregation, degradation, oxidation, denaturation and the like of the recombinant fusion protein effectively so as to retain bioactivity and is suitable to be used in clinic.
CN101015566A Combined treatment method for type 2 diabetes by using camel milk and rosiglitazone maleate The invention is to use camel milk and rosiglitazone maleate for combined treatment of type II diabetes, and relates to the field of medicine. It was reported that camel milk can reduce trypsin dosage for patients with type I diabetes mellitus. But there is no report about the effect of camel milk on type II diabetes. The experiment of the invention indicates that drinking camel milk alone has the same effect with rosiglitazone maleate in reducing blood sugar, blood lipid, and trypsin. Combined drinking of rosiglitazone maleate 4mg and camel milk 8ml once each day has better therapeutic effect than exclusive use of rosiglitazone maleate in reducing blood sugar, blood lipid, and trypsin. The invention has the advantages of convenient administration and low cost, and also is benefit for the economical development of pastoral zone.
US20080182823 E.g., polyethylene glycol-linked alendronate or pamidronate; osteoporosis, osteopenia, urolithiasis, hypercalcemia, Paget's disease, bone metastasis, multiple myeloma, or neoplastic bone lesion The present invention provides for methods of administering a bisphosphonate active agent to a subject in need thereof. Aspects of the invention include administering the bisphosphonate active agent to the subject by a pulmonary route, where the bisphosphonate active agent is bonded, either directly or through an intervening linking group, to a non-peptide polymer, such that the bisphosphonate active agent is a polymer-linked-bisphosphonate active agent. Also provided are compositions for use in practicing methods according to embodiments of the invention. Methods and compositions according to embodiments of the invention find use in a variety of different applications, including but not limited to, the treatment of bone adsorption disease conditions.
US6908914 Antipsychotic cyclic N-aralkylamines The invention relates to benzene derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of psychotic disorders.
US7825228 Bone mineralization proteins, DNA, vectors, expression systems The present invention is directed to isolated nucleic acid molecules that encode LIM mineralization protein, or LMP. The invention further provides vectors comprising nucleotide sequences that encode LMP, as well as host cells comprising those vectors. Moreover, the present invention relates to methods of inducing bone formation by transfecting osteogenic precursor cells with an isolated nucleic acid molecule comprising a nucleotide sequence encoding LIM mineralization protein. The transfection may occur ex vivo or in vivo by direct injection of virus or naked plasmid DNA. In a particular embodiment, the invention provides a method of fusing a spine by transfecting osteogenic precursor cells with an isolated nucleic acid molecule having a nucleotide sequence encoding LIM mineralization protein, admixing the transfected osteogenic precursor cells with a matrix and contacting the matrix with the spine. Finally, the invention relates to methods for inducing systemic bone formation by stable transfection of host cells with the vectors of the invention.
CN101006846A Anti-stress nutrition additives for poultry and its preparation method Disclosed is an irritability-resistant nourishing additive for fowls and process for preparation, wherein the additive is prepared from the following constituents (by weight portions) through mixing homogeneously: water-soluble vitamin A 20.0-60.0 parts, water-soluble vitamin D3 40.0-90.0 parts, water-soluble vitamin E 100.0-120.0 parts, vitamin K3 powder 4.0-7.0 parts, vitamin B1 1.0-5.0 parts, vitamin B2 1.0-7.0 parts, vitamin C powder 5.0-15.0 parts, calcium pantothenate 5.0-10.0 parts, and folic acid 0.1-1.0 part, potassium chloride 30.0-70.0 parts, sodium chloride 30.0-50.0 parts, borneol 1.0-10.0 parts, waterless glucose 1255.0-1935.0 parts.
CN103251607A Application of Myriberine A in preparation of medicines for treating or preventing yellow fever virus infection The invention discloses an application of Myriberine A in preparation of medicines for treating or preventing yellow fever virus infection. The Myriberine A can effectively inhibit yellow fever virus from multiplication, but has small toxicity to cells, can be further developed to prepare the medicines for treating diseases caused by virus infection and has a wide application prospect. The application of Myriberine A in preparation of medicines for treating or preventing yellow fever virus infection is disclosed for the first time, a framework type belongs to a brand-new framework type, the Myriberine A has an unexpected strong effect of inhibiting the yellow fever virus activity, and the revelation possibility of other compounds cannot be generated, so the application has obvious substantive features; and moreover, the application has an obvious improved effect of preventing the yellow fever virus infection.
EP2528600A1 Dry powder pharmaceutical composition comprising tiotropium and fluticasone The present invention relates to pharmaceutical compositions in dry powder form comprising tiotropium and fluticasone propionate and/or their pharmaceutically acceptable derivatives as active agents, and capsule and blister forms containing these pharmaceutical compositions so as to be used in treatment of respiratory tract diseases.
CN101095679A Granisetron hydrochloride orally disintegrating tablets The invention relates to granisetron hydrochloride mouth slaking tablet and the formula and preparing process. The process employs rotary oscillating granulator to produce said slaking agent through direct sheeting method after heat extrusion by melting and gradient cooling. When compared with mouth slaking agent produced with normal melting method, the mouth slaking agent in this invention is characterized by faster slaking speed, higher dissolution rate, intact tablet outlook, stronger rigidity and good taste. If compared with current freeze drying, vacuum drying, spray drying technique, the invention is characterized in that it needs no special production device and condition, no special package, the production process is simple, quality is stable and suitable for industrial production. It provides new products for patients that is dysphagia and bedridden, for old people and children, especially for patients suffering tumor chemotherapy and radiotheraphy.
US20060154874 Treatment of symptoms associated with bacterial vaginosis The invention relates to the use of saccharide, such as lactose for the preparation of a medicament for the treatment and/or prophylaxis of one or more symptoms caused by bacterial vaginosis, wherein the medicament comprises at least 20 percent by weight of saccharide, and wherein the medicament is substantially free from bacteria. Furthermore, the invention relates to a method for treating one or more symptoms associated with bacterial vaginosis, as well as a pharmaceutical composition comprising the saccharide.
CN101375858A Solid formulation of urea nitrogen sorbent for compensating kidney function and preparation method thereof The invention relates to a solid prepration which is used as a blood urea nitrogen absorbent for compensating the renal function. The combination of raw materials and the weight ratio are as follows: the raw materials comprise 50-80 percent of coated aldehyde oxystarch, 1-20 percent of wetting agent sodium alginate, 1-30 percent of dispersant and 0.1-5 percent of curing agent. The dispersant is selected from one or more of gelatin, Arabic gum, carboxymethyl cellulose, hydroxypropyl methyl cellulose and ethyl cellulose; and the curing agent is soluble calcium salt or aluminium salt solution. The solid preparation can be powder, capsules, tablets and other solid preparations which can be realized on the pharmacy. The preparation has the targeting role of the coated aldehyde oxystarch, the action part is in the intestinal duct, the drug system absorbs water in the intestinal duct and precipitates the sodium alginate under the condition that the pH is equal to 7-9, the viscosity of the sodium alginate is larger, the flow of the sodium alginate in the intestinal duct is slow, and then the residence time of the drug in the intestinal duct is prolonged, thereby improving the efficacy for carrying out the full absorption of nitrogen and ammonia in the intestinal duct.
US20080207538 Enhanced Production of Functional Proteins From Defective Genes This invention provides methods for enhancing production in a subject of a functional protein from a gene disrupted by a mutation, for example by the presence of a premature stop codon or by an exon skipping mutation, comprising administering to the subject an amount of an agent effective to suppress the mutation and an amount of an agent effective to increase transcription of the gene.
CN1927399A Application of non-nucleoside virus reverse transcriptase inhibiting compound and derivative thereof for anti-hepatitis B virus purpose The invention relates to an application of non-nucleosides restrain virus inverse-transfer enzyme compound (KM-1) and derivate, in the medicine production. Wherein, the KM-1 can be used in anti-hepatitis virus replication. The invention uses autogenous polymer enzyme active restrain test technique, and the anti-hepatitis virus gene transfer dye cell research replication technique, to build the platform that testing the naphthalenesulfonic acid compound KM-1 anti-hepatitis virus replication; and uses the KM-1 in different densities to restrain HBV replication. The inventive KM-1 and derivate can be used to prepare the anti-virus infection medicines as acute hepatitis B, etc.
CA2843359A1 Monoamine oxidase inhibitors and methods for treatment and diagnosis of prostate cancer A mechanism of monoamine oxidases (MAOs) driven epithelium-to-mesenchymal transition (EMT) is disclosed. Also disclosed are methods for treating cancer by inhibiting or suppressing MAOs in cancer cells. Novel MAOs inhibitors, such as small molecules, siRNA, shRNA, antisense oligonucleotides, aptamers, decoys, and pharmaceutical compositions useful for treating cancer by disrupting the workings of MAOs are provided. In particular, a class of conjugates formed by covalently conjugating near infrared dye 783, IR-780, and MHI-148 to a MAO inhibitor, such as clorgyline, with and without encapsulation it in a nanoparticle is provided. Other aspects of the invention include methods for forming the nano-conjugates, method for monitoring treatment progress in a cancer patient by monitoring the changes in MAO activity, methods for screening patients who are at risk of cancer or differentiating different forms of cancer by assaying the level and location of MAO activity.
US7329753 Quinoline and isoquinoline derivatives, a process for their production and their use as inflammation inhibitors The invention relates to quinoline and isoquinoline derivatives of general formula I and a process for their production, and their use as inflammation inhibitors.
CN101352442A Sustained release tablets containing cefaclor active component and preparation method thereof The invention discloses a sustained-release preparation containing the active ingredient of cefaclor, which consists of the cefaclor, acrylics II, slow release stroma of hydroxypropyl methylcellulose, cementing agent, loading agent and other supplementary materials; wherein, the proportion by weight among the cefaclor, the slow release stroma and the acrylics II is 1:0.1-1:0.01-0.1. After being taken, the cefaclor sustained-release tablets can be slowly and continuously released according to the requirements to maintain effective blood level, thus achieving the action of controlled release. The sustained-release preparation has the characteristics of lasting action, low toxic and side effect, few times for taking medicine, and utilizing the minimum dose to achieve the best healing efficacy; furthermore, blood concentration is stable, the incidence rate of untoward effect is reduced, and the sustained-release preparation is more applicable to the use of the patients.
US7119120 A 2-benzenesulfonylamino-N-benzyl-benzamides for treating hyperphosphatemia, urogential disorders Disclosed are compounds which have been identified as inhibitors of phosphate transport. Many of the compounds are represented by Structural Formula (I): Ar1—W—X—Y—Ar2; or a pharmaceutically acceptable salt thereof. Ar1 and Ar2 are independently a substituted or unsubstituted aryl group or an optionally substituted five membered or six membered non-aromatic heterocylic group fused to an optionally substituted monocylic aryl group. W and Y are independently a covalent bond or a C1–C3 substituted or unsubstituted alkylene group. X is a heteroatom-containing functional group, an aromatic heterocyclic group, substituted aromatic heterocyclic group, non-aromatic heterocyclic group, substituted non-aromatic heterocyclic group, an olefin group or a substituted olefin group. Also disclosed are methods of treating a subject with a disease associated with hyperphosphatemia, as well as a disease mediated by phosphate-transport function. The methods comprise the step of administering an effective amount of the one of the compounds described above.
CN101712675A Nitrogenous benzheterocycle derivate and application thereof to treating nervous and mental diseases The invention discloses a nitrogenous benzheterocycle derivate and application thereof to treating nervous and mental diseases. Pharmacology experiments show that the derivate has better anti-schizophrenia action and lower toxicity. The derivate is free alkali or salt having the following structure general formula.
US7220399 Alpha or beta emitters attached to fragments in radioimmunotherapy The present invention relates to radioimmunoconjugates useful in targeted radioimmunotherapy and methods of treating a patient using radioimmunoconjugates. The radioimmunoconjugates of the present invention comprise an alpha- or beta-emitting radioisotope and a binding site linked to or on an antigen-binding fragment of an antibody which specifically binds to a tumor-associated antigen. The methods of treating a patient can include administering one or more clearing agents to the patient in conjunction with the radioimmunoconjugate of the present invention, as well as subsequently grafting bone-marrow or autologous stem-cells to the patient.
US7435739 Antiproliferative agents; skin, prostate glands, kidneys, central nervous system The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.
CN103751125A Domperidone orally disintegrating tablet and preparation method thereof The invention provides a domperidone orally disintegrating tablet, which is characterized in that the tablet contains a physiologically effective amount of domperidone and a necessary pharmaceutically applicable excipient; the weight percent of domperidone in the orally disintegrating tablet is 5%-10%, and the pharmaceutically applicable excipient is a mixture of a plurality of agents selected from fillers, odor masking agents, disintegrants, surfactants, adhesives, lubricants, and glidants. The domperidone orally disintegrating tablet provided by the invention has the advantages of quick disintegration, excellent mouthfeel, stable quality, and reliable curative effects, and can improve the compliance of medicine taking for patients.
US20120129824 Pharmaceutical Formulations Containing Corticosteroids for Topical Administration The potency of a topical corticosteroid in a pharmaceutical formulation is maintained even when the concentration of the corticosteroid is substantially reduced by providing the corticosteroid in a formulation containing a liquid oil component that includes a dicarboxylic acid ester and/or a monocarboxylic acid ester.
WO2011015523A1 Benzyl-substituted tetracyclic heterocyclic compounds The present invention pertains to Benzyl-substituted tetracyclic heterocyclic compounds, as well as the resulting pharmaceutical compositions, and their use in the treatment or prophylaxis of diseases alleviated by inhibition of type 5 phosphodiesterases. Furthermore, the present invention pertains to the methods of manufacturing these Benzyl-substituted tetracyclic heterocyclic compounds.
EP0994655B1 Satiety product A food composition giving a prolonged feeling of satiety, comprising a mixture of or an oil-in-water emulsion of triglyceride oils having a solid fat content at ambient or body temperature with a food emulsifier. The invention also refers to the use of said mixture or oil-in-water emulsion for the preparation of a pharmaceutical composition for the control of calorie or fat intake.
EP2702985A1 Equol Level Regulator An object of the invention is to provide a medical drug, a food and drink having a role in regulating the concentration of equol in vivo and being capable of taking for a long time with high safety and provide a selective medium for a microorganism having conversion ability to equol and a method of detecting the same. Provided are an equol concentration-raising or reducing agent containing a carbohydrate as an active ingredient; use of a carbohydrate for producing the equol concentration-raising or reducing agent; a method of raising or reducing the concentration of equol by administrating a carbohydrate in an effective dose; a selective medium containing a carbohydrate for a microorganism having conversion ability to equol; and a method of detecting a microorganism having conversion ability to equol by use of the selective medium.
CN102552313A Compound vitamin E nicotinic acid ester nanoemulsion The invention discloses compound vitamin E nicotinic acid ester nanoemulsion, which is composed of the following raw materials by mass percent: vitamin E nicotinic acid ester 0.68%-7.06%, dextro sugar anhydride sulfate sodium 0.50%-5.00%, vitamin C 0.50%-5.00%, a surface active agent 20.59%-38.00%, assist surface active agent 0-13.07% and oil 2.50%-9.06%, and allowance is distilled water. The sum of the mass percent of the raw materials is 100%. The compound vitamin E nicotinic acid ester nanoemulsion is colorless or light yellow transparent liquid, has the advantages of being good in stability, strong in dispersity, good in permeability, high in biological utilization and the like, enables curative effect of the medicine to be reinforced, and enables toxicity of the medicine to be reduced. Three medicines are compounded to have the effect of comprehensively treating hyperlipidemia and arteriosclerosis. Simultaneously, the compound vitamin E nicotinic acid ester nanoemulsion is low in production energy consumption, high in safety and capable of being produced in mass.
EP2654637A1 Kit-in-parts for cleaning and treating ears of companion animals The invention relates to a kit-in-part comprising of a composition for the use as a cleaning and treating of ears of a companion animal and suitable packaging material, wherein the kit-in part additionally consists of components selected from the group of a pharmaceutical composition for use in the treatment of otitis externa, application and dosage information, cannules, cotton swabs, gauzes and information about the cleaning and maintenance ears of a companion animal.
US20080213400 Combinations of Chromium with Antidiabetics for Glucose Metabolism Disorders Compositions and methods of using the same for the treatment of diabetes and other disorders of glucose metabolism are provided. Compositions may include an anti-diabetic agent and one or more of a bioavailable source of chromium and vanadium.
CN101095681A Alfuzosin Hydrochloride permeating pump type controlled-release preparation and method for preparing the same The invention belongs to medical technique field, and relates to osmotic pump controlled-release tablets of alfuzosin hydrochloride and the preparation method, which comprises tablet core, clothing sheet membrane and controlled-release pore. The solid medicine and osmotic active substance and shaping agent forms the tablet core; the coating membrane is insoluble controlled-release clothing sheet that is water permeable but not medical permeable. Said pore is on the clothing sheeting membrane. The comprised raw material of tablet core and clothing sheet membrane and proportion by weight are as follows: table core: alfuzosin hydrochloride 0.5-50%, packing agent 5-80%, penetration -promoting agent 5-80%, lubricating agent 0.2-3%, adhesive agent 0.01-10%; clothing sheet membrane: semi-permeable membrane clothing sheet high polymer material 70-99%, plasticizing agent 1-30%. The invention is characterized by stable and continuous release, long retention time for effective blood concentration and reduced peak-to-valley of blood concentration phenomena.
US20120021012 Novel pharmaceutical uses for nanoparticles The present invention relates to SiC nanoparticles to be used in the context of cancer treatment, said nanoparticles preferably having a size less than 100 nm.
CN1534010B Water soluble extract of red sage root and its preparation method and use A water-soluble extract of red sage root containing danshinolic acid B, danshensu and proshikonic acid, its preparing process, and its application in preparing the angiotonin converzyme depressant medicines for treating hypertension, and hypertension accompanied by heart failure or diabetes or nephrosis are disclosed.
WO2007054580A1 N-sulfamoyl-n’-benzopyranpiperidines as inhbitors of carbonic anhydrases The present invention relates to novel N-sulfamoyl-N'-benzopyranpiperidines of general formula (I) and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the prophylaxis and/or treatment and/or prevention and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and its concomitant and/or secondary diseases or conditions.
WO2011121418A1 4 - aminopyrimidine derivatives and their as as adenosine a2a receptor antagonists New 4-amino-pyrimidine derivatives as potent antagonists of the adenosine A2a receptor formula (I): (I) The invention provides as well a method for preparing such compounds, pharmaceutical compositions comprising an effective amount of these compounds and the use of such compounds in the manufacture of a medicament to treat pathological affections that can be improved by antagonism of the adenosine A2a receptor.
US20100136072 Polymeric Coatings that Inactivate Viruses and Bacteria Hydrophobic polymeric coatings which can be non-covalently applied to solid surfaces such as metals, plastics, glass, polymers, textiles, and other substrates such as fabrics, gauze, bandages, tissues, and other fibers, in the same manner as paint, for example, by brushing, spraying, or dipping, to make the surfaces virucidal and bactericidal, have been developed.
US20070248698 Obesity and Metabolic Syndrome Treatment with Tanshinone Derivatives Which Increase Metabolic Activity The present invention relates to a composition for preventing and treating metabolic syndrome, containing tanshinone derivatives as an effective ingredient. More specifically, the present invention relates to a composition for preventing and treating metabolic syndrome, containing tanshinone derivatives that exhibit superior activity in enhancing metabolic activity, as an effective ingredient.
CN101822679A Cefepime hydrochloride combined medicament The invention discloses a cefepime hydrochloride combined medicament, which removes medicament heat and anaphylactic reaction of cefepime hydrochloride and adverse reactions thereof on liver damage, injection pain, phlebitis produced by injection and the like in the prior art. The cefepime hydrochloride combined medicament has the advantages of safe use, stable quality and reliable curative effect. A preparation process for the medicament is energy-saving, environmentally-friendly and pollution-free.
CN103044460A 3,5,7-triphenyl-5H-thiazolo[3,2-a]pyrimidin derivatives and application thereof The invention discloses 3,5,7-triphenyl-5H-thiazolo[3,2-a]pyrimidin derivatives of the general formula I or pharmaceutically acceptable hydrates and salts thereof, including stereisomers or tautomers thereof, wherein R1, R2 and R3 can be optionally selected by one or two independently from hydrogen, hydroxyl, nitryl, acetyl, halogen, C1-C6 alkyls, C1-C6 alkoxyls, C1-C10 arbitrarily and selectively substituted amino alkoxyls and C1-C10 arbitrarily and selectively substituted or unsubstituted amino formacyl alkoxyls. The 3,5,7-triphenyl-5H-thiazolo[3,2-a]pyrimidin derivatives according to the invention have obvious inhibition effect on cyclin dependent kinases, thus the derivatives can be applied to treatment and prevention of various diseases such as cancers of human and animals.
CN1994299A Use of medicine for treating virus infection of respiratory system The invention relates to a method for producing drug that treats virus infection of respiratory tract, wherein it uses Arbidol Hydrochloride as 6-bromine-4-(dimethylamino)-5-hydroxyl group-1-methyl-2-(benzene sulfenyl)-1H-indole-3-glycolate-hydrates. The invention can reduce the mouse dead rate affected by virus B3, B5, adenovirus, etc, and improve antibody level, with wide application.
US20100249095 Substituted Spiro-amide Compounds Substituted spiro-amide compounds corresponding to formula I in which R5 through R8, D, X, Y and Z have defined meanings, processes for preparing such spiro-amide compounds, pharmaceutical compositions containing such compounds, and methods of using such spiro-amide compounds for treating and/or inhibiting disorders or disease states mediated at least in part by the bradykinin 1 receptor.
WO2005084681A1 Composition for increasing levels of hormones and a method for preparation of said composition The present invention includes a pharmacologically acceptable composition for ingestion by a mammal, having a first ingredient including a hormone or a substance which stimulates production of a hormone, such as testosterone or growth hormone. The composition also may include a second ingredient which stimulates the production of cyclic GMP. The second ingredient may also be Morinda citrifolia or an extract thereof. The composition of the present invention increases levels of a hormone with a body.
EP2585079A1 Semuloparin for the extended prevention of a mortality and/or morbidity event in a patient having undergone hip fracture surgery The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof for the extended prevention of a mortality and/or morbidity event, more specifically venous thromboembolism and death, in a patient having undergone hip fracture surgery.
EP1733758A1 Methods for administration of a farnesyl dibenzodiazepinone This invention relates to compositions and methods for inhibiting growth and proliferation of a neoplastic cell, and methods of treating neoplasms in a mammal using the compound of Formula I or a pharmaceutically acceptable salt, prodrug thereof. More particularly, the invention relates to the use of the compound of Formula I as a continuous intravenous infusion administrable preparation for the treatment of neoplastic disorders.
CA2767339A1 Pharmaceutical compositions and therapeutic methods employing a combination of a manganese complex compound and a non-manganese complex form of the compound A pharmaceutical composition for treatment of a pathological condition in a patient comprises, as a first component, a manganese complex of Formula I(), and, as a second component, a non-manganese complex compound of Formula (I), optionally together with one or more physiologically acceptable carriers and/or excipients, wherein X, R, R, R, and R are as defined herein. Methods for treatment of a pathological condition in a patient, for example, a pathological condition caused by the presence of oxygen- derived free radicals, comprises administering to said patient the first component and the second component.
WO2013011932A1 Azabenzimidazole derivative having ampk-activating activity Provided is a compound useful as an AMPK activator. A compound represented by formula (wherein R4 represents a hydrogen atom or a substituted or unsubstituted alkyl group; R1, R2 and R3 independently represent a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, a nitro group, a carboxy group, a substituted or unsubstituted alkyl group, or the like, wherein a case in which R1, R2 and R3 represent a hydrogen atom simultaneously is excluded; X represents a single bond, -S-, -O-, -NR5-, -C(=O)-, or the like; R5 represents a hydrogen atom, or a substituted or unsubstituted alkyl group; and Y represents a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted cycloalkenyl group, a substituted or unsubstituted heterocyclyl group, or the like), or a pharmaceutically acceptable salt thereof.
WO2007114827A1 Substituted heterocyclic compounds and methods of use The present invention relates to compounds having the general structure: (I) and pharmaceutically acceptable salts and hydrates thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
CN102379933A Epidemic prevention drug and use method thereof The invention relates to an epidemic prevention drug and a use method thereof. The manufacturing method comprises the steps as follows: mulling rhizoma atractylodis, realgar, rhubarb into powder, placing the powder in wine, and storing the mixture hermetically. The epidemic prevention drug is prepared simply, is economical and practical, has an obvious effect, and can improve self resistibility of a human body and effectively prevent epidemic situation from spreading without restriction.
WO2014057179A1 Use of xenon to prevent or treat the neurological consequences of a septic shock The invention concerns a gaseous composition containing gaseous xenon for use by inhalation in order to prevent or treat at least one neurological consequence secondary to a septic shock in a patient.
US20110152375 Method of reducing the methane gas level and of increasing the total gas yield in animal feed The present invention relates to the use of at least one porous metal-organic framework material (MOF) comprising at least one first and, if appropriate, one second organic compound, where at least the first organic compound binds coordinatively to at least one metal ion in an at least partly bidentate manner, where the at least one metal ion is Mg(II) and where the first organic compound is derived from formic acid and the second organic compound from acetic acid, for reducing the methane level in the total gas produced, and to the use for increasing the total gas formation during feed digestion in ruminants as well as a method for reducing the methane level in the total gas produced and a method for increasing the total gas formation during feed digestion in ruminants.
WO2010067008A3 Bicyclic derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics The invention relates to compounds having formula (I) wherein: R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 represents a hydroxyl group, a thiol group, a (C1-C4)alkyloxy group or a thio(C1-C4)alkyl group; and n is an integer equal to 1 or 2, in the form of a base or acid addition salt, as well as in hydrate or solvate form. The invention also relates to the preparation method thereof and to the use of same in therapeutics.
EP2343314A2 Calcium fluoride phosphopeptide complexes The present invention relates to novel complexes in which amorphous calcium fluoride phosphates are stabilised by phosphopeptides. The complexes have anti-cariogenic effects and may also be used as dietary supplements to increase calcium bioavailability and to heal or prevent diseases associated with calcium deficiencies.
WO2007009393A1 The use of chlorogenic acid in the manufacture of medicaments for increasing the effect of bone marrow cells The use of chlorogenic acid in the manufacture of medicaments for increasing the effect of bone marrow cells . The pharmaceutical composition comprising chloroginic acid as active component . Chlorogenic acid can treat anaemia caused by many reasons , which comprise , but not to limited , blood loss anemia , hemolytic anemia , anhematopoietic anemia which include megaloblastic anemia , aregenerative anemia , and hypersplenia , as well as leucopeina , granulocytopeni and agranulocytopenia caused by many reasons , the change of macronucleus system casued by many reasons , for example , idiopathic thrombocytopenic purpura ; myelofibrosis , bone marrow infection caused by many reasons .
CN103070857A Application of butylphthalide The invention discloses an application of a known compound (butylphthalide) in preparing a drug for treating dysmenorrhea or an application in preparing a drug for preventing the dysmenorrhea. Related experiments indicate that butylphthalide has a good treating and preventing effect on the dysmenorrhea; and as butylphthalide has the advantages of good toleration, no obvious accumulation, high pharmacological activity and low adverse effect, butylphthalide is a very promising drug for treating and preventing the dysmenorrhea.
CN103202803A Imiquimod vesicle gel and preparation method for same The invention relates to an imiquimod vesicle gel and a preparation method for the same. The vesicle gel is obtained by preparing a vesicle suspension by using imiquimod and the nonionic surfactants of Brij, Span, Poloxamer and the like via self-assembly, then reacting with the mixed gel matrix of carbomer and povidone, and used for treating the diseases of exophytic genital warts, actinic keratosis, skin basal cancer, melanoma and the like via local application on the skin; and by adding povidone in the carbomer gel matrix, the in-vitro medicine release amount can be increased by 42.1%, thus being beneficial to promote the entrance of medicines in the skin to exert the functions. According to the imiquimod vesicle gel and the preparation method for the same disclosed by the invention, the intradermal retention volume of the medicines in 24 hours can be remarkably increased and is 2.1 times that of the commercially available emulsifiable pastes, and the dose of the medicines penetrating through the skin is reduced by 48.7%; and the equivalent intradermal retention volume can be achieved only by a half of the dose of the commercially available emulsifiable pastes, so that the effectiveness of the medicine effect of the medicated parts can be remarkably enhanced, the dose of the medicines entering in the body can be greatly reduced, and the toxic and side effects of the whole body can be reduced.
CA2172392C Methods of inhibiting phagocytosis The present invention relates, in general, to methods of treating diseases resulting from interactions between immune complexes and Fc receptors. In particular, the present invention relates to methods of modulating the clearance of antibody-coated cells from the circulation by inhibiting phagocytosis and to methods of modulating the interaction of immune complexes with tissue Fc receptors. Further, the invention relates to methods of modulating the activation of immunological processes mediated by Fc receptor activation resulting from antibody-antigen/receptor interaction.
US20120322862 Aptamers to 4-1BB and Their Use in Treating Diseases and Disorders The present disclosure relates generally to the field of nucleic acids and, more particularly, to aptamers capable of binding to 4-1BB; pharmaceutical compositions comprising such 4-1BB aptamers; and methods of making and using the same.
WO2013056183A1 Polymorphs of arry-380, a selective herb2 inhibitor and pharmaceutical compositions contianing them Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.
US20090068199 Methods for Treating and Detecting Beta-Cell Disease The role of synaptic adhesion molecules in human cell development and function is largely unknown. This invention provides methods to study β-cell function in native tissue through the use of novel adhesion and migrations assays. Through the use of these assays, the inventors have been able to for the first time describe the contribution of SAMs to human β-cell adhesion, spreading, and motility. Furthermore, the inventors have used the results of these assays to develop methods for detection, treatment, and prevention of diseases related to the pancreas.
US20090203711 Inhibitors of P38 Map Kinase Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is —N═ or —CH═; B is an optionally substituted divalent mono- or bicyclic aryl or heteroaryl radical having 5-13 ring members; R2 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z-L1-Y1—R wherein A, z, Y1, and L1 are as defined in the specification; R is a radical of formula (X) or (Y) wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; and D is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring D is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring.
EP1267843B1 System for transporting active substances in a biological system The invention relates to a stabilizer-free system for transporting active substances in a biological system, consisting of one or more active substances and magnetic particles. The inventive system is characterized in that the particles are provided with active substances on at least part of their surface. The magnetic particles do not necessarily have to be modified in this system. The system can be incorporated into aqueous and oily suspensions, as well as in microemulsions, oil-in-water emulsions, water-in-oil emulsions and water-in-oil-in-water emulsions.
CN102256973A Corydaline derivatives useful for reducing lipid levels The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL- cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated potein kinase.
EP2772252A1 Oxybutynin-containing transdermal absorption preparation A transdermal absorption preparation containing at least one drug selected from oxybutynin and pharmaceutically acceptable salts thereof and 0.05% by mass or more of a sterol selected from cholesterols, cholesterol derivatives and cholesterol analogs, relative to a total amount of the transdermal absorption preparation.
US20100297181 AMPA Receptor Antagonists for Epilepsy, Mental Disorders or Deficits in Sensory Organ The invention provides methods for treating epilepsy, mental disorders and/or deficits in sensory organ by administering to patients therapeutically effective amounts of AMPA receptor antagonists in combination with one or more other active ingredients useful for treating epilepsy, mental disorders and/or deficits in sensory organ. The invention also provides pharmaceutical combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists, and optionally, one or more other active ingredients that are useful for treating epilepsy, mental disorders and/or deficits in sensory organ.
US7407975 Epothilone derivatives, method for producing same and their pharmaceutical use This invention relates to the new epothilone derivatives of general formula I, in which substituents Y, Z, R2a, R2b, R3, R4a, R4b, D-E, R5, R6, R7, R8 and X have the meanings that are indicated in more detail in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanomas, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (psoriasis, arthritis). To avoid uncontrolled proliferation of cells and for better compatibility of medical implants, they can be applied or introduced into polymer materials. The compounds according to the invention can be used alone or to achieve additive or synergistic actions in combination with other principles and classes of substances that can be used in tumor therapy.
CN101987859A Aryl ammonia sulphonyl sulphonate derivative of glucocorticoid The invention relates to an aryl ammonia sulphonyl sulphonate derivative of glucocorticoid and discloses a compound shown as a formula (II). In the formula (II), X is C1-12-dialkane, CpF2p group, monocycle or bicyclo C3-8-dinaphthenic optionally substituted by halogen atoms, hydroxyl or nitrile, monocycle, bicyclo or tricyclo C6-15-arylene optionally substituted by halogen atoms, hydroxyl, nitrile or alkyl, hetero dialkane with 1 to 6 carbon atoms and substituted carbon atoms comprising one or more identical or different heteroatoms, C1-4-dialkane aryl, C1-4-dialkane-C3-8-naphthenic base or C3-8-dinaphthenic-C1-4-alkyl, wherein p is 1 to 5; and Drug is optionally substituted glucocorticoid forming sulphonate through OH group.
CN1969849A Stable pharmaceutical composition containing pitavastatin calcium and preparation process thereof The invention discloses a drug composition and making method of stable calcium Bimvastatin, which comprises the following parts: 0.01-10% calcium Bimvastatin, 10- 93% filler, 1-30% disintegration agent, 0.01-5% lubricant and 0.1-80% alkali findings.
US20060142255 Hypocholesteremic preparations containing phytostenolesters of conjugated fatty acids, and methods of reducing serum cholesterol levels using the same A hypocholesteremic preparation containing at least one phytostenol ester of a conjugated fatty acid having from about 6 to about 24 carbon atoms is disclosed. Methods of reducing serum cholesterol content in a mammal via administration of hypocholesteremic preparations described herein are also disclosed.
WO2005074942A1 Slow release steroid composition A pharmaceutically acceptable composition comprising an anti-inflammatory steroid or pharmaceutically acceptable salt thereof, which exists in varying crystal and crystal composite sizes wherein the proportion of crystals and crystal composites above 20 µm in size in the composition is greater than the proportion of crystals and crystal composites under 20 µm in size.
WO2008051440A1 Crystal modifications -3- (1h-ind0l-3-yl) -4- [2- (4-methyl-piperazin-1-yl) -quinazolin-4-yl] -pyrrole-2, 5-d ione The invention relates to a new crystalline form of the acetate salt of, 3-(1.H.-indol-3-yl)-4-[2-(4-methyl-piperazin-1-yl)-quinazolin-4-yl]-pyrrole-2,5-dione, which may be used for example for transplantation.
WO2009151392A1 Novel derivatives of 11-piperazin-l-yldibenzo [b,f] [1,4] thiazepine for treating at least one syndrome or condition associated with schizophrenia and other psychotic disorders This invention relates to novel compounds having the structural Formula I below: (I) and their pharmaceutically acceptable salts or tautomers, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence and neurodegenerative disorders.
CN103239431A Compound ambroxol hydrochloride composition capsule and preparation method thereof The invention relates to the field of pharmacy and discloses a compound ambroxol hydrochloride composition capsule. 1000 granules of drugs are prepared from the following active ingredients: 7.0-8.0g of ambroxol hydrochloride, 1.5-2.5g of salbutamol sulfate, 160-170g of microcrystalline cellulose, 2.5-3.5g of sodium carboxymethyl starch and 1.5-2.5g of silicon dioxide. The compound preparation formed by ambroxol hydrochloride and salbutamol has the beneficial effects that through synergistic action of the two drugs, the functions of expelling phlegm to arrest coughing and resisting asthma can be simultaneously achieved, the cough symptom can be quickly relieved and sputum removal can be promoted; secretions and bronchospasm accompanying asthma and acute and chronic bronchitis can be better controlled by using the two drugs jointly; and through drug combination, not only are the lung functions improved but also the number of asymptomatic days of patients is increased, and the life quality of the patients is improved. The invention also discloses a preparation method of the compound ambroxol hydrochloride composition capsule. The preparation method is simple in process and is suitable for industrial production.
CN103059035A Application of composition of fugu extract, evening primrose oil and flax seed oil to toxin removal of human body The invention provides application of a composition comprising alkaloids extracted from viscera of fugu (Fugu vermicularis), evening primrose oil and flax seed oil to removal of medicine residues, chemical residues, pesticide residues and heavy metal residues in human body. The invention is characterized in that the composition has reasonable proportion of total alkaloids, evening primrose oil and flax seed oil, and can significantly improve the immunity of the human body, and clear harmful ingredients in human body.
WO2008107436A1 Bicyclic organic compounds suitable for the treatment of inflammatory or allergic conditions A compound of formula (I): in free or salt form, wherein A, R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.
WO2007109561A1 Immunomodulatory saccharide compounds Compounds comprising a saccharide molecule and a 5-deoxy-5-methylthio-xylofuranose (MTX) moiety or a 5-deoxy-5-methylsulfoxy-xylofuranose (MSX) moiety, and use of such compounds in methods for modulating inflammation and immune responses.
EP1536839B1 Combination therapy comprising omega-interferon for treating infection with hepatitis c virus or yellow fever virus A method of treating an immunologic, proliferative, or infectious disease in a warm-blooded animal is disclosed. The method comprises administering to the animal omega interferon (IFN) at a dosage and activity for the disease state treated sufficient to induce a therapeutic response in the animal, which dosage and activity for the disease state treated is higher than would be well-tolerated based on data for non-omega IFN's. The omega IFN is administered alone or in combination with a therapeutically effective amount of at least one adjunctive therapeutic agent. Also disclosed is an article of manufacture useful for treating an immunologic, proliferative, or infectious disease, which article comprises (1) omega IFN in a from suitable for administering a therapeutically effective amount of the omega IFN to the subject in order to induce the desired therapeutic response (2) instructions for administering the omega IFN as desired, that is higher than would be well-tolerated based on data for non-omega IFNs.
CN102573994A Novel bicyclic urea compounds The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer
US7507407 Immunoliposomes that optimize internationalization into target cells The present invention provides for immunoliposomes that optimizes internalization of a drug into target cells bearing a characteristic cell surface marker. The immunoliposomes comprise an Fab′ domain of an antibody that specifically binds the characteristic marker, an amphipathic vesicle-forming lipid, and a polyethylene glycol derivatized lipid. The invention also provides for growth-inhibiting immunoliposomes that lack growth-inhibiting therapeutic agents and yet are capable of inhibiting the growth and proliferation of target cells.
CN100594909C Therapeutic agent for hemorrhoidal disease An external preparation containing acetylsalicylic acid or its pharmaceutically acceptable salt as an active ingredient for treating anal diseases having therapeutic activity on hemorrhoids (internalhemorrhoid, external hemorrhoid), hemorrhoidal disease owing to anal fissure and other anal diseases together with activity on pain and pruritus.
WO2011012885A9 Fulvestrant in a dosage of 500mg for the treatment of advanced breast cancer The present invention relates to fulvestrant at a dosage of 500mg for use in the treatment of a postmenopausal woman with advanced breast cancer who has progressed or recurred on endocrine therapy.
CA2383027C Apparatus and method for anesthetizing the cervical region of a female A novel and useful apparatus for delivering an anesthetic locally to the cervical region of a female is provided, wherein the apparatus comprises a ring (1) having a surface (5) and at least one depression (2) on the surface (5). An anesthetic composition comprising an anesthetic agent and an excipient are placed within the at least one depression (2). The ring (1) is comprised of a pharmaceutically acceptable inert material that is biocompatible. Furthermore, the ring (1) is of sufficient size that it can be inserted into the vaginal canal of a female. In the vaginal canal, the anesthetic agent is immediately released from the anesthetic composition and directly anesthetizes the cervical region.
WO2011152485A1 Novel 4,5-fused pyrimidine derivative Disclosed is a 4,5-fused pyrimidine derivative which is useful as a pharmaceutical product. Specifically disclosed is a pyrimidine derivative which is effective for prophylaxis and/or treatment of diseases associated with signaling mediated by a toll-like receptor (TLR).
WO2014043792A1 Glucosamine pro-drugs To develop glucosamine (GlcN) pro-drugs with properties superior to the presently available GlcN products, we have synthesized derivatives with improved pharmaceutical properties. The synthesized derivatives include peptide-GlcN ester conjugates where the peptide portion consists of one or more amino acids. One such compound is (5-amino-3,4,6-trihydroxyoxan-2-yl)methyl 2-(2-aminoacetamido)-3-methylbutanoate or glycine-valine-COO-GlcN (GV-GlcN).
CN103735523A Peretinoin medicinal composition The invention provides a peretinoin medicinal composition. The medicinal composition is a peretinoin dropping pill preparation, and comprises active medicine peretinoin and a matrix. The dripping drill is prepared by heating and melting the medicine and the matrix, dripping into a condensate which cannot be uniformly mixed with the medicine and the matrix, concentrating and condensing to prepare the preparation. The peretinoin medicinal composition can be kept stable for a long time, and is quick in drug release, simple in production equipment and convenient to operate.
US20130023588 Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques.
DE102005045146A1 Antimicrobial preparation useful for treating e.g. wound, eczema and vaginal infections comprises octenidine dihydrochloride encapsulated in liposomes An antimicrobial preparation (C1) comprises octenidine dihydrochloride encapsulated in liposomes. An independent claim is included for manufacture of the antimicrobial preparation (C1) involving mixing water at elevated temperature with phospholipid and octenidine dihydrochloride, and homogenizing the mixture. - ACTIVITY : Vulnerary; Dermatological; Gynecological; Antimicrobial; Fungicide; Antibacterial. In vitro cytotoxicity of a preparation (A) comprising (wt.%) Phospholipon 90 H (RTM: phospholipid) (b1)(6), octenidine dihydrochloride (0.05), octyldodecanol (15), alpha -DL-tocopherol (0.5), pentylene glycol (5) and water (73.45) was tested against mouse fibroblast cell line L929 (ATCC CCL1). Evaluation took place with the aid of two different spectrophotometric methods. With the comparative preparation without (b1), 50% of the test cells were not vital after exposure to 32 mu g/ml (method 1) and 41.3 mu g/ml (method 2) for 30 minutes. The preparation (A) showed a cytotoxicity of less than 20% even at the highest concentration possible in the test, of 250 mu g/ml octenidine dihydrochloride. - MECHANISM OF ACTION : Microbial growth inhibitor.
WO2008049984A3 Use of citrulline for treating undernutrition conditions The present invention relates to the use of L-citralline (I) or a pharmaceutically acceptable salt thereof for preparing a drug for the treatment of undernutrition conditions related to a decrease in protein synthesis in the case of pathologies that do not result from an enteric deficiency. (I)
US20070213402 Compounds which interact with the thyroid hormone receptor for the treatment of fibrotic disease A method of alleviating a fibrotic disease selected from systemic sclerosis and muscular dystrophy in a warm blooded animal, which comprises administering an effective amount of at least one compound having the formula (I) in which X, n, R1 and R2 have the meanings given in the specification.
WO2008104161A1 ß-CARBOLINES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES The invention relates to derivatives of 9-alkyl-ß-carboline, the production thereof, and pharmaceutical compositions comprising said derivatives of 9-alkyl-ß-carboline. The invention further relates to the use of said derivatives of 9-alkyl-ß-carboline and said pharmaceutical compositions for the treatment and prevention of locomotion disorders, neurodegenerative diseases, Alzheimer's disease, and Parkinson's disease. These effects may furthermore be made useful for the cultivation of cells such as, for example, dopaminergic cells or stem cells to be transplanted for the treatment of Parkinson's disease.
CN101269026A Ornidazole sustained-release dropping pill and preparation method thereof The invention discloses a drug containing sustained-release ornidazole drug and used for treating infections of trichmonad, amoeba, giardia and anaerobic organism in gynecopathy as well as the preparation method thereof. The drug aims to provide a sustained-release ornidazole dropping pill formulation which has excellent curative effect, low toxic and side effects, broad-spectrum antibacterium, safer use, low frequency of drug taking and long effective hours and is prepared by adopting the solid dispersion technology, thereby thoroughly changing the defects existing in conventional oral formulations from the drug structure. The sustained-release ornidazole dropping pill adopts ornidazole as the ingredient and is prepared jointly with the medicinal carrier used as the stroma.
CN101606910B Ceftizoxime sodium drug injection powder and preparation method thereof, as well as synthetic method of bulk drug ceftizoxime sodium The invention relates to a ceftizoxime sodium drug injection powder and a preparation method thereof, as well as a synthetic method of bulk drug ceftizoxime sodium. The ceftizoxime sodium drug injection powder consists of 100% ceftizoxime sodium, wherein the ceftizoxime sodium is pretreated, and the pretreatment is aseptic refining and/or grinding. The ceftizoxime sodium drug has the advantages of high purity, almost no impurity, better and more stable quality, better clarity and the like; and the synthetic method of bulk drug ceftizoxime sodium has lower bulk cost, less synthesis technology difficulty, mild reaction condition, stable and reliable yield and quality, and high purity and yield of products.
WO2009113109A1 New phenanthrylphenol linked pyrrolo[2,l-c][l,4]benzodiazepine hybrids as potential antitumour agents and process for the preparation thereof The present invention provides a compounds of general formula (6), useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo [2,1-c] [l,4]benzodiazepine hybrids of general formula (6).
WO2009034386A1 Derivatives of adenine and 8-aza-adenine and uses thereof-796 The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I): which have bacterial MurI inhibitory activity and are accordingly useful for their treatment and prophylaxis of bacterial infection, e.g., E.faecalis or E. faeciuminfection. Further, the invention relates to methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of the compounds, to pharmaceutical compositions containing them, and to their use in the manufacture of medicaments of use in the treatment and prevention of various bacterial diseases in a warm-blooded animalsuch as man.
WO2013175805A1 Ghrelin receptor agonists for the treatment of achlorhydria The present invention relates to a use of a compound having ghrelin receptor agonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for treatment of diseases including achlorhydria in which abnormal gastric acid secretion is involved. In addition, the present invention relates to the method of treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agents. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound of the present invention or a pharmaceutically acceptable salt thereof for the treatment of said diseases.
US7396841 Injections An injectable composition comprises a benzimidazole compound having an antiulcer action and a strong alkali (e.g., an alkali metal hydroxide such as sodium hydroxide) in a proportion of about 1 equivalent of the latter relative to 1 mol of the former, and is substantially free from a nonaqueous solvent. The injectable composition may comprise N-methylglucamine, and a saccharide (such as mannitol). The injectable composition may be a freeze-dried preparation. The freeze-dried preparation is dissolvable in or dilutive with a distilled water for injection or an infusion solution without a nonaqueous solvent. The injectable composition is useful as an antiulcer agent.
CA2759275A1 Microencapsulated compositions and methods for tissue mineralization The present invention is directed to compositions, products and methods useful for bone and tooth mineralization. The compositions comprise polymer microcapsules containing aqueous salt solutions. The shells of the microcapsules can be semi- permeable or impermeable. Solutions of calcium, fluoride and phosphate salts are particularly useful in the compositions of the invention. The microcapsules are preferably prepared by surfactant free inverse emulsion interfacial polymerization. Bone products include cements, scaffolds and bioactive glass. Dental products include pastes, gels, rinses and many other dental materials.
EP1549310A1 Gelled laxative compositions The invention provides orally administered gelled formulations comprising a laxative which is active in the digestive tract.
US7122530 24-hydroxyvitamin D, analogs and uses thereof The invention provides 24-hydroxyvitamin D compounds and methods for their use in the treatment and prophylaxis of hyperparathyroidism and hyperproliferative diseases, and in the modulation of the immune and inflammatory responses as well as the treatment of bone depletive disorders.
US20100048639 Oxadiazole derivates as s1p1 receptor agonists The present invention relates to novel oxadiazole compounds of formula (I) having pharmacological activity, pharmaceutical compositions containing them and their use in the treatment of various disorders.
WO2011077313A1 Piperidinecarboxamides as mpges - 1 inhibitors The invention relates to piperidinecarboxamides of formula (I), to their use in medicine as mPGES-1 inhibitors for the treatment of pain, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
US20060052457 Use of ppar alpha agonists for the treatment of vascular and renal diseases Activation of peroxisome proliferator activated receptor alpha (PPARα) by administration of therapeutic amounts of a PPARα agonist, WY-14643, inhibits the proliferation of vascular smooth muscle cells, hepatoma cells and human renal proximal tubule cells. WY-14643 may be applicable as a medicament for the treatment of proliferative vascular disease (atherosclerosis, hypertension), revascularization-induced injury (restenosis) and chronic renal failure.
US7718695 Inclusion compounds of fumagillol derivative or its salt, and pharmaceutical compositions comprising the same The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.
WO2011084725A1 4-AMINO-2-(ETHOXYMETHYL)-1-(2-HYDROXY-2-METHYLPROPYL)-1H-IMIDAZO[4,5-c]QUINOLIN-5-IUM 1-HYDROXYNAPHTHALENE-2-CARBOXYLATE COMPOSITIONS AND METHODS A compound of formula:[ I ] Pharmaceutical compositions containing the compound, and methods of inducing cytokine biosynthesis in an animal, treating a viral infection and/or treating a neoplastic disease in an animal by administering an effective amount of the compound to the animal are also disclosed.
US20060040910 Macrocycles useful in the treatment of Alzheimer's disease The present invention are macrocycles of the formula (IX): for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
US20110293534 Aerosol can spray incorporating a nutritional cell scaffold for use as first aid treatment for wounds/burns and for use in cell therapy/tissue repair A First Aid aerosol can spray using a propellant authorized for human use. Spray will be in the form of a ‘light emulsion’ for use on burns and wounds at incident sites. If propellant is not used, two of the spray constituents, namely sterile cornstarch granules, a nutritional cell scaffold and antibiotic(s) may be used for guided subcutaneous tissue repair. Specific cell culture techniques are described for both epidermal and dermal cells which are to be externally applied to aid wound healing of wider, deeper wounds/burns in terms of total body area affected.
CN101072773A Pyrrole derivatives having CRTH2 receptor antagonist activity There are provided according to the invention compounds of formula (I) as CRTh2 antagonists. In free or salt form, wherein R<3>, R<4>, R<5>, R<6>, Q, W and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.
US7723080 Murine α (1,3) fucosyltransferase Fuc-TVII, DNA encoding the same, method for preparing the same, antibodies recognizing the same, immunoassays for detecting the same, plasmids containing such DNA, and cells containing such a plasmid A gene which encodes a murine leukocyte α(1,3)fucosyltransferase capable of synthesizing the sialyl Lewis x determinant has been cloned.
US6919316 Administering to a subject in need, an immunosuppressively effective amount of at least one sulfofucosylacylglycerol compound An immunosuppressive agent comprising, as an effective ingredient, at least one compound selected from the group consisting of compounds represented by general formula (1) below and pharmaceutically acceptable salts thereof: wherein R101 represents an acyl residue of a higher fatty acid, and R102 represents a hydrogen atom or acyl residue of a higher fatty acid.
CN102836122A Composition injection containing meptazinol hydrochloride, and preparation method thereof The present invention discloses a composition injection containing meptazinol hydrochloride, and a preparation method thereof. Per 1000 ml of the composition injection comprises 115.6 g of the meptazinol hydrochloride, 1.0 g of sodium bisulfite, and 0.5 g of calcium disodium edetate. During preparation, a prescription amount of the meptazinol hydrochloride is weighed, and is added with 85% of water for injection to dissolve the meptazinol hydrochloride; the sodium bisulfite and the calcium disodium edentate are added, and stirring is performed to completely dissolve; and a 0.2 mol.L<-1> sodium hydroxide solution is adopted to adjust the pH value to 5.5-6.0. The drug composition of the present invention has characteristics of good and simple production process, easy performing, inexpensive and available raw materials, and good stability.
US20120269890 Process for obtaining a rosuvastatin calcium composition and obtained product The present invention describes a rosuvastatin calcium composition that does not require tribasic phosphate salts to be stable and that also has suitable bioavailability, and is helpful in reducing lipid and/or cholesterol levels in the body, as well as the manufacturing method of this composition.
EP2164840A2 Modulators of cftr Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette ('ABC') transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ('CFTR'). The present invention also relates to methods of treating CFTR mediated diseases using compounds of the present invention.
CA2258679C Solid solution of an antifungal agent with enhanced bioavailability A pharmaceutical composition in the form of a substantially amorphous solid solution comprising an antifungal compound of formula (I), wherein X is F; and R1 is formula (1) or an ester or ether of said compound of formula (I); and a soluble or insoluble polymer such as: povidone or crospovidone, wherein the ratio of said compound to said polymer is about 1:3 to about 1:6 is disclosed.
US20110236486 Method to produce hyaluronic acid functionalized derivatives and formation of hydrogels thereof A system and method are provided for controlling an internal combustion engine driving a generator/welder or a stand-alone generator. Controlling the engine may include altering the engine speed based upon a detected demand on the generator and/or operating parameters of a welder. For example, the engine speed may be increased based on a detected draw on the generator and/or the operating parameters of the welder. In addition, the engine speed may be automatically decreased to a non-standard idle speed or the engine may be automatically turned off if no demand is detected for a period of time. Additionally, the engine speed may be increased if only frequency-insensitive demands are detected on the generator. Combinations of these and further methods may be executed. Various devices are provided for implementing the above methods.
US20120077792 Lanthanide metal complexes useful in treating cancer The present invention relates to a compound of formula (I). Provided is also a method of killing a cell that comprises administering the compound of formula (I). Provided is also a method of treating cancer or diabetes in a mammal that comprises administering the compound of formula I and respective pharmaceutical compositions thereof.
EP1480961B1 Glutaminyl based dpiv inhibitors The present invention provides a compound of the formula (I): wherein X = CH2 or S or a pharmaceutically acceptable salt thereof. Such compounds and their corresponding pharmaceutically acceptable acid addition salt forms, are useful in treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.
EP1994932A1 Use of N-desmethylclozapine to treat human psychosis Disclosed herein is a method to treat psychosis. Treatment is carried out by administering a therapeutically effective amount of N-desmethylclozapine to a patient suffering from psychosis.
US20140057995 Aqueous-lipidic carotenoid-containing compositions The invention provides a primary carotenoid-containing composition comprising an aqua-containing component, a lipid-containing component and a carotenoid-containing fiber material from plant origin with lowered content of aqua-soluble substances. The invention also provides oral compositions that comprise the primary composition in a foodstuff, in a food supplement or in a pharmaceutical preparation.
WO2008068615A1 Crystalline forms of ( 3 s ) -3- [n- (n' - (2-tert-butylphenyl) oxamyl) alaninyl] amino-5- (2 ', 3 ', 5 ', 6 ' -tetrafluoro phenoxy) -4-0x0penta noic acid The present invention relates to crystalline forms of (3S)-3-[N-(N'-(2-tert- butylphenyl)oxamyl)alaninyl]amino-5-(2',3',5',6'-tetrafluorophenoxy)-4-oxopentanoic acid (see formula (I)). The invention further relates to pharmaceutical compositions comprising such crystalline forms and to the use of said pharmaceutical compositions and said crystalline forms in the treatment of various conditions, particularly in the treatment of liver fibrosis.
WO2006049148A1 1β-METHYLCARBAPENEM DERIVATIVE A carbapenem derivative which is highly effective in the treatment or prevention of microbism, in particular, infectious diseases of the respiratory system. It is a carbapenem compound represented by the general formula [Chemical formula 1] (I) [wherein A is optionally substituted C1-6 alkyl, substituted C2-4 alkenyl, C3-6 cycloalkyl, an optionally substituted C4-6 heterocyclic group, monosubstituted amino, or disubstituted amino; n is 1 or 2; and X is oxygen or sulfur] or a pharmacologically acceptable salt or ester derivative of the compound.
EP1871363A1 Combined-step process for pharmaceutical compositions The invention relates to a process for the solid oral pharmaceutical formulation of a pharmaceutically active ingredient such as levetiracetam, comprising a wet granulation of the pharmaceutically active ingredient and simultaneous fluid bed drying such that, as the pharmaceutical blend granulates it is simultaneously dried thus preventing it from becoming a paste. The invention therein thus provides a novel formulation preparation process characterized by a 'combined' Granulation and Fluid Bed Drying process step.
US20100209384 Sustained release formulations comprising very low molecular weight polymers The present invention relates to a parenteral, sustained and controlled release, semisolid formulation comprising an end-capped oligomer and at least one active substance without any supplementary viscosity reducing agent or excipient.
CN103446078A Method for administrating preparations containing oseltamivir guanidyl carboxylate analogues and/or ethyl esters thereof The invention relates to a method for administrating preparations containing oseltamivir guanidyl carboxylate analogues and/or ethyl esters thereof. Administration is carried out through inhalation. The method can be used for treating cold caused by influenza viruses. By adopting the administration method provided by the invention, not only can dependence on the single variety of drugs such as oseltamivir, zanamivir and peramivir be reduced and new drug resistant virus strains generated by using the single variety in quantity be avoided but also the method which is favorable for greatly improving the bioavailability compared with oral administration or intravenous drip is provided for oseltamivir guanidyl carboxylate analogues or ethyl esters thereof; more importantly, the method which has the advantages of small drug dose, less side effects and high effect taking speed is provided.
US20120094996 Imidazo [2, 1-B] [1, 3, 4] Thiadiazole Derivatives There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.
EP1463487A4 Liposomal delivery of vitamin e based compounds The present invention provides a method for treating a cell proliferative disease by delivering a composition comprising a vitamin E based anti-cancer compound contained within a delivery vesicle of an individual in need of such treatment where the compound has a structural formula where R' is a hydrogen or a carboxylic acid; R2 and R3 are hydrogen or R4; R4 is methyl; and R5 is alkyl. Also provided is a vesicle comprising these compounds.
CN1785174A Application of wogonin for preparing medicine to treat or prevent hepatitis B An application of wogonin in preparing the medicines for preventing and treating hepatitis B by suppressing the copying of HBV DNA and the secretion of s and e antigens of hepatitis B and decreasing the content of HbsAg in serum is disclosed.
WO2008097646A1 Methods to treat and/or prevent mucositis The present invention relates to methods useful for treating and/or preventing mucositis using an active vitamin D compound.
CN1935119A Clopidogrel sulfate solid preparation, and its preparing method The present invention relates to a solid preparation of clopidogrel hydrochloride and its preparation method. It is characterized by that in said sold preparation the palmitoleostearin and micropowder silica gel are added, and its preparation method adopts a grinding equivalent progressively-increasing method so as to raise the stability and safety of said solid preparation.
US20120289525 Pyrimidine ether derivatives and methods of use thereof The present invention relates to Pyrimidine Ether Derivatives, compositions comprising a Pyrimidine Ether Derivative, and methods of using the Pyrimidine Ether Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
US8796298 Combination of a B-Raf inhibitor: N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1- dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide and the Akt inhibitor: N-{ (1S)-2-amino-1-[(3- fluorophenyl)methyl]ethyl}-5-chIoro-4-(4-chIoro- 1 -methyl- 1 H-pyrazol-5-yl)-2-10 thiophenecarboxamide useful in the treatment of cancer The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
US20100297082 Weight-bearing polyurethane composites and methods thereof Present inventions present composites of particles and polymers, as well as methods of making such composite and uses thereof. A low or non-porous composite comprises a plurality of bone particles; and polyurethane components with which the bone particles are combined. Provided composites can be prepared in a one-shot process. Alternatively or additionally, composites can be prepared by compression molding under a high pressure. Before or after implantation, provided composites may be set to form a hardened state of composites that provides mechanical strength and supports the in-growth of cells.
US20070264319 Transdermal Antiemesis Delivery System, Method and Composition Therefor A transdermal antiemesis system, preferably in the form of a drug-in-adhesive matrix patch, is disclosed comprising an effective antiemesis amount of a selective serotonin (5-HT3) receptor antagonist as an antiemetic incorporated in a skin adhesive composition containing at least one permeation enhancer and a water-insoluble pressure-sensitive adhesive. A preferred antiemetic is granisetron base. The transdermal antiemesis system of this invention provides controlled release of the active antiemetic ingredient from the skin-contacting adhesive formulation of a transderrnal patch, and maintains a sustained transdermal delivery of the antiemetic.
US20130259905 Composition capable of inducing endoplasmic reticulum stress A composition capable of inducing endoplasmic reticulum stress including nanogold particles and a solvent is disclosed. After a chronic myelogenous leukemia patient intakes the composition capable of inducing endoplasmic reticulum stress, the endoplasmic reticulum stress of the chronic myelogenous leukemia cells is induced to cause apoptosis and cell death, so as to alleviate and control chronic myelogenous leukemia.
US20050049268 Use of at least one abl, kit and/or platelet-derived growth factor receptor tyrosine kinases inhibitor for treating hair depigmentation The invention relates to a method of treating a warm-blooded animal, especially a human, having depigmented hair or subject to hair depigmentation comprising administering to the animal a useful amount of a) at least one Abl, Kit and/or platelet-derived growth factor (PDGF) receptor tyrosine kinases inhibitor, the use of a) and at least one cosmetic acceptable carrier, to retard, prevent, suppress, and/or revere the depigmentation of hair, the use of a) for the preparation of a medicament for the treatment of a disease characterized by hair depigmentation and a topical cosmetic composition comprising a useful amount of at least one Abl, Kit or PDGF receptor tyrosine kinases inhibitor.
CN101396342A Anti-cancer sustained-released injection containing epothilone derivate The invention relates to an anti-cancer sustained release injection containing epothilone derivative, consisting of sustained microspheres and menstruum. The sustained microspheres comprise anti-cancer drugs selected from taxane, alkylating agent and/or plant alkaloid and the like, the epothilone derivative and sustained release auxiliary material. The menstruum is a special menstruum containing suspending agent. The epothilone derivative is selected from epothilone B, epothilone D, iso-epothilone D, BMS-247550, azaepothilone B, furan epothilone D or BMS-310705. The sustained release auxiliary material is selected from poly-dl-lactide, the glycolic acid copolymer of the poly-dl-lactide, polyethyleneglycol, the polylactide copolymer of the polyethyleneglycol, carboxyl terminated polylactide copolymer, fatty acid and decanedioic acid copolymer, etc. The suspending agent is selected from carboxymethyl cellulose and the like with the viscosity of 100cp to 3000cp (under the temperature of 25 DEG C to 30 DEG C). The sustained release microsphere can also be made into a sustained release implant. The sustained release injection is injected or arranged in or around the tumour and can release drug at partial position for 40 days approximately, therefore, the sustained release injection improves the local drug concentration selectively and enhances the treatment effect of non-operative treatments, such as radiotherapy, chemotherapy and the like at the same time.
CN101591340B 5,10,15,20-tetra-(5-drewamine amyl)-chlorin, preparation and application thereof in field of medicaments and pesticides The invention relates to 5,10,15,20-tetra-(5-drewamine amyl)-chlorin. A chemical structural formula is shown as the formula (I). Preparation of the 5,10,15,20-tetra-(5-drewamine amyl)-chlorin comprises the following steps of: using pyrrole and 6-chlorine-1-hexanal as raw materials; under the action of Lewis acid, adding tetrachlorobenzoquinone for oxidation and organizing; preparing an important intermediate of 5,10,15,20-tetra-(5-amyl chloride)-porphin; performing the displacement reaction of the intermediate and different bisacetamidt; eluting the residuals by silica gel column chromatography; performing the reduction reaction of the residuals and a reducer; removing a solvent from the product; and separating and eluting the product to obtain the 5,10,15,20-tetra-(5-drewamine amyl)-chlorin. The compound has good fat solubility and water solubility, high selective absorption in a tumor cell, so that the compound is an ideal photosensitizer; and the synthetic route has the advantages of simple operation, low cost, environmental protection and good economic benefits and application prospect.
CN203342089U Arnebia root oil-immersed spunlace nonwoven fabric paste for external use The utility model relates to arnebia root oil-immersed spunlace nonwoven fabric paste for external use and belongs to medical dressing. The arnebia root oil-immersed spunlace nonwoven fabric paste for external use comprises an isolation cloth, a mucilage glue layer, a spunlace nonwoven fabric and arnebia root oil, and the arnebia root oil-immersed spunlace nonwoven fabric paste for external use is technically improved in the aspects that the mucilage glue layer is adhered to the inner side of the isolation cloth, the arnebia root oil is immersed to the spunlace nonwoven fabric, and the spunlace nonwoven fabric is fixedly bonded on the isolation cloth. By virtue of the technical improvements, the arnebia root oil-immersed spunlace nonwoven fabric paste for external use has the beneficial effects that the isolation cloth is waterproof and can separate oil, so that wounded skin can be prevented from touching water and the arnebia root oil can be prevented from permeating clothes; the mucilage glue layer can directly paste the arnebia root oil-immersed spunlace nonwoven fabric paste onto skin, thus a patient can move conveniently, and the arnebia root oil-immersed spunlace nonwoven fabric paste is prevented from slipping off.
EP2768316A1 Lipid composition for the prevention or treatment of skin problems The invention relates to a novel lipid composition. Further, the invention relates to the use of a lipid composition for the treatment, alleviation and prevention of skin problems.
US20050049229 Antiinflammatory and/or antiplatelet aggregation actions; lower toxicity, reducing liver and/or kidney damage; analgesic and antipyretic activity 2-Hydroxyacetanilide may be formulated for use in medicine as a therapeutic or prophylactic agent for application as an anti-inflammatory and/or an anti-platelet aggregation drug.
WO2013134867A1 Therapeutic regimens and methods for improving visual function in visual disorders associated with an endogenous retinoid deficiency Therapeutic regimes for improving visual function in a subject having a deficiency in endogenously produced 11-cis retinal comprising administering the synthetic retinal derivative as a divided dose over 2-7 days then providing a resting period of 7-28 days after which the second dose of the synthetic retinal derivative is administered. Preferred synthetic retinal derivatives are 9- or 11-cis-retinyl esters. Disorders associated with deficiency in endogenously produced 11-cis retinal include retinitis pigmentosa and Leber congenital amaurosis.
CN101440085A Thrombin inhibitors containing guanidine heterocyclic compound and preparation thereof The invention belongs to the field of chemical synthesis, and relates to a thrombin inhibitor containing a guanidyl heterocyclic compound and a preparation method thereof. The method constructs a basic group which has high affinity to thrombin active sites, synthesizes a compound which has anticoagulation effect and the following structural formula, and can prepare a direct thrombin inhibitor. A target compound obtained by the method is subjected to activity test, and the result shows that the target compound has obvious inhibition effect on the generation of thrombin. The method for synthesizing the thrombin inhibitor has simple step operation and separation, shorter route and higher yield in various steps, and used reagents are all commonly used reagents.
WO2014027857A1 Composition comprising alpha-iso-cubebene or alpha-iso-cubebenol as active ingredient for preventing or treating infectious or inflammatory diseases The present invention relates to a composition comprising alpha-iso-cubebene or alpha-iso-cubebenol as an active ingredient for preventing or treating infectious or inflammatory diseases. The alpha-iso-cubebene or alpha-iso-cubebenol according to the present invention exhibits excellent effects and protective mechanisms in a preclinical mouse model of sepsis, and therefore can be effectively used in preventing or treating infectious or inflammatory diseases.
US20080004310 Lyophilized pharmaceutical composition A stable pharmaceutical composition with increased solubility that includes at least one lyophilized compound that is papaverine, phentolamine or alprostadil.
EP1237552B1 Combination of lumilysergol and riluzole for preventing and/or treating motoneuronal diseases The invention concerns the use of a combination of an ergoline selected among nicergoline and lumilysergol and riluzole or one of its pharmaceutically acceptable salts for preventing and/or treating motor neuron diseases.
EP2641602A1 Method for treating gynecological diseases The present invention relates generally to a combination for use in the treatment of gynaecological diseases and associated disabling symptoms thereof, in a subject in need thereof, said pharmaceutical combination for use comprising co-administering a suitable pharmaceutical composition for oral administration comprising a first progesterone receptor modulator and a pharmaceutical composition suitable for vaginal and/ or intrauterine administration comprising a second progesterone receptor modulator.
US20110142931 Soft tablet containing dextrose monohydrate The invention relates to a tablet capable of being chewed or disintegrated in the oral cavity, which comprises a pharmaceutically active ingredient, and a matrix comprising directly compressible dextrose monohydrate and sucralose, said tablet being substantially fat free and said matrix being substantially free of non-saccharide, water soluble polymeric binders.
CN103271880A Cefodizime sodium injection and preparation method thereof The invention relates to a cefodizime sodium and preparation method thereof, especially relates to a cefodizime sodium injection for treating microbe infection, and preferably relates to a freeze-drying powder injection. The cefodizime sodium injection of the present invention is mainly composed of active component cefodizime sodium and accessories such as mannitol and citric acid. The solvent in the injection of the present invention is injection water; the excipient in the freeze-drying powder injection is mannitol, and sodium hydroxide or hydrochloric acid is used for adjusting pH valve.
WO2007055513A1 Quinazoline derivatives as a signal transduction inhibitor and method for the preparation thereof The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof as a signal transduction inhibitor, a method for the preparation thereof, and a pharmaceutical composition and a therapeutic composition comprising same as an active ingredient. The inventive quinazoline derivative as a signal transduction inhibitor can selectively and effectively inhibit diseases caused by the overactivity of a tyrosine kinase.
WO2014039920A1 Administration of acetylcholinesterase inhibitors to mitigate neurotoxin-induced paralysis and residual neuromuscular blockade Methods and kits for treating or reducing the likelihood of neurotoxin-induced respiratory failure in a subject, such as a victim of neurotoxic envenomation are provided. Also provided are methods for treating or reducing the likelihood of residual neuromuscular blockade in a subject to whom a nondepolarizing neuromuscular blocking agent has been administered. The methods involve administering a pharmaceutically effective dose of an acetylcholinesterase inhibitor to the subject, where the administration is not via injection. In some embodiments intra-nasal or ocular administration is used.
US20100063001 Microbial-derived chondroitin sulfate Described is chondroitin sulfate obtained from microbial sources, and related compositions and methods.
US20100179153 Bicyclic S1P Receptor Modulators The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, b their use as medicaments and to medicaments comprising them.
CN103242336A Gambogic acid-type derivative and preparation and application thereof The invention relates to a gambogic acid-type derivative and preparation and application thereof. The derivative is shown as formula I, formula II and formula III, wherein R1 is H or nitrogen heterocyclic ring or -(CH2)mR3, m is 1-8, R3 is nitrogen heterocyclic ring or NR4R5, R4 and R5 are respectively selected from H and C1-8 linear-chain or branch alkyl groups, or the R4 and R5 form a loop, R2 is a H, alicyclic or nitrogen heterocyclic ring, and X is O or NH independently or forms the nitrogen heterocyclic ring together with R1. The preparing method comprises the step of enabling the gambogic acid catalyzed and rearranged under medium-strong protonic acid to react with R1XH or salt compound thereof. The gambogic acid-type derivative disclosed by the invention has broad-spectrum antitumor activity, has obvious grow inhibiting effect on multiple solid tumors, can form salt compound to greatly improve water-solubility, is stable in chemical structure and is expected to be developed as an innovative antitumor medicine.
CN101411772A Method for preparing teeth-strengthening powder The invention provides a method for preparing tooth fixing powder which is a tooth fixing medicine for eliminating swell and pain of gum and halitosis, and preventing the loosening and falling-off of teeth. When the tooth fixing powder is used to brush teeth, the tooth fixing powder can make the smooth circulation of qi blood, relieve bruises and pains, prevent the loosening of teeth and make the teeth not suffered from tooth diseases for ever.
CN1806575A Method for preparing liver-benefiting, face-beautifying yoghout with micron pine pollen, pearl powder for women The invention relates to a process for preparing liver-benefiting and face-beautifying yoghourt, which is prepared from various conventional soymilks and air flow super fine disintegrated micrometer pine pollen powder, micron pearl powder, micrometer ligustrum japonicum powder, micrometer lotus nut starch, micrometer doddor seed powder, micrometer wolfberry fruit powder, oligosaccharide and other intestinal tract-benefiting bacterium as raw materials through combination fermentation. The invention realizes the functions of liver-benefiting, face-beautifying, blood circulation-promoting, pain-relieving, fatigue-resisting, and human body immunity-improving.
CN1743337A Taxol derivative and its pharmaceutical composition The invention relates to pacilitaxel derivative in whose formula cholesterol is jointed on to the hydroxyl-group of pacilitaxel structure. Pacilitaxel and cholesterol chlorocarbonate are used as raw material directly reacting to prepare the said derivative. This invention also discloses medicinal composition using the derivative as active component, especial a lipid nano particle preparation, and the use of which in preparing medicine for treating and preventing tumor.
CN102362857A Dexibuprofen injection and preparation method thereof The invention discloses dexibuprofen injection and a preparation method thereof. The invention is characterized in that the injection is preparation which is prepared by using dexibuprofen as the main ingredient. The preparation consists of dexibuprofen, meglumine, citric acid and trisodium citrate. The pH value of the solution is 5.0 to 7.0. The preparation has the advantages that: dexibuprofen acts quickly and is absorbed quickly; the medicinal liquid directly enters blood circulation without being affected by the digestion system and foods; and the like. The stability of the injection is high.
CN103204813A Condensed imidazole derivatives as TRPV3 antagonist The invention provides a transient receptor potential vanilline (TRPV) modifier having a structure represented by formula (I). The above compounds can be used for treating or preventing TRPV3 adjusted diseases, illnesses and/or obstacles. The invention also provides preparation methods of the compounds, intermediates used in the synthesis of the compounds, pharmaceutical compositions of the compounds, and a method for treating or preventing the TRPV3 adjusted diseases, illnesses and/or obstacles.
US20130090516 Local Anesthesia By Magnet-Directed Concentration of Nanoparticle Conjugated Anesthetic Methods and formulations for induction of local anesthetic effects employing magnetic nanoparticles conjugated to anesthetic molecules. Magnetic nanoparticle-local anesthetic conjugates may be safely injected intravenously into human and animal subjects without encountering the deleterious effects observed with traditional injections of local anesthetics. The magnetic nanoparticle-local anesthetic conjugate may be concentrated at a site of action through the application of an external magnetic field to the patient at a site where local anesthesia is desired.
US7456171 Nicotinic ligands; treatment of nervous system disorders, neurodegenerative disorders, psychological disorders, and tobacco, drug and alcohol withdrawal symptoms The present invention discloses and claims compounds of general formula in which X represents a nitrogen atom or a group of formula C—R2, P represents a group of formula C—R3, Q represents a group of formula C—R4, R represents a group of formula C—R5, W represents a group of formula C—R6, or one of the symbols P, Q, R and W represents a nitrogen atom, R1 represents a hydrogen atom or an alkyl group, R2 represents a hydrogen atom or an alkyl group, R3, R4, R5 and R6 each represent a hydrogen or halogen atom, or an alkyl, alkoxy, nitro, amino, trifluoromethyl, cyano or amino group or other functional groups. The compounds of the invention are useful in a variety of therapeutic applications.
WO2012075111A1 Uses of anti-cd40 antibodies in combination therapy for b cell-related cancers This invention relates to new uses of anti-CD40 antibodies in combination with bendamustine in the treatment of diseases or conditions associated with neoplastic B-cell growth. The invention is particularly useful for the treatment of patients who have previously been administered (i) the chimeric anti-CD20 monoclonal antibody rituximab, or (iii) combination therapy with rituximab and a chemotherapeutic regimen.
CN103655581A Application of bile acid series derivatives in anti-tumor metastasis drugs The invention belongs to the invention field of compound medicine use, and discloses the effect of bile acid series derivatives in inhibiting the growth of tumor cells. According to the invention, 4'-hydroxybutylcholate having the highest activity is screened out from the bile acid series derivatives; and on this basis, the anti-tumor metastasis effect of the 4'-hydroxybutylcholate is further determined by various detection methods.
CN101530412A Pharmaceutical composition of blonanserin and preparation method thereof The invention discloses a [2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5, 6, 7, 8, 9, 10- hexahydro-cycloocta-(b) pyridine), a composition of salts thereof for medical purposes and a preparation method thereof. The pharmaceutical composition has such a stabilizing agent as alkaline substance with a weight not less than 10 percent. The composition has good stability and can block a 5-hydroxytryptamine-2 acceptor and a dopamine-2 acceptor and be applied to the treatment of schizophrenia.
CN102132952A Folium cortex eucommiae common melastoma herb cigarette and preparation method thereof The invention relates to a folium cortex eucommiae common melastoma herb cigarette and a preparation method thereof. The folium cortex eucommiae common melastoma herb cigarette is characterized by being prepared by processing prepared folium cortex eucommiae in the Cili county of Hunan province, liquorice filament, common melastoma herb leaves, any one of tea oil and vegetable oil, honey and stalactite fine particles. The folium cortex eucommiae common melastoma herb cigarette comprises the following components in percentage by weight: 45-55 percent of folium cortex eucommiae, 10-20 percent of liquorice, 45-55 percent of common melastoma herb leaves, 0.5-1 percent of any one of tea oil or vegetable oil and 0.5-1 percent of honey. The preparation method comprises the following steps of: placing the folium cortex eucommiae into a pot for frying, wherein the process is called as green removal; placing the folium cortex eucommiae into a machine for kneading; taking out and placing the folium cortex eucommiae into a drier for drying to obtain processed folium cortex eucommiae; taking the aired dry liquorice and cutting the liquorice into filaments in 1-2mm by using a machine for later use; picking the common melastoma herb leaves in summer and autumn; cleaning with clear water, leaching and airing or drying for later use; and cleaning picked stalactite, removing farraginous stone, grinding into fine particles by using a machine and airing for later use.
US20100196365 Use of imidazoquinolines for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members The present invention relates to the use of compounds of formula (I) in the treatment of Epidermal Growth Factor Receptor (EGFR) family members dependent diseases or diseases that have acquired resistance to agents that target EGFR family members, use of said compounds for the manufacture of pharmaceutical compositions for the treatment of said diseases, combinations of said compounds with EGFR modulators for said use, methods of treating said diseases with said compounds and pharmaceutical preparations for the treatment of said diseases comprising said compounds alone or in combination, especially with an EGFR modulator.
CN101601383A Exotic plant Eupatorium adenophorum Spreng effective ingredient caffeic acid intercalated hydrotalcite and preparation method The invention provides exotic plant Eupatorium adenophorum Spreng effective ingredient caffeic acid intercalated hydrotalcite and a preparation method, and belongs to the field of pesticides or medicaments. The structural formula of the exotic plant Eupatorium adenophorum Spreng effective ingredient caffeic acid intercalated hydrotalcite is M1-xMx(OH)2(C9H8O4)x.mH2O. The exotic plant Eupatorium adenophorum Spreng effective ingredient caffeic acid intercalated hydrotalcite is an anionic supermolecular stratified material formed by separating exotic plant Eupatorium adenophorum Spreng effective ingredient caffeic acid by a counter current chromatography, reacting to replace NO3 among precursor hydrotalcite laminate panels by an ionic exchange method. The method has the advantages that the exotic plant Eupatorium adenophorum Spreng effective ingredient caffeic acid with pesticide or medicament characteristics is assembled among the hydrotalcite laminate panels to realize effective storage of the hydrotalcite for the exotic plant Eupatorium adenophorum Spreng effective ingredient and achieve the slow release performance of the hydrotalcite on the ingredient, thereby providing the novel 'storage-release' method of the hydrotalcite applied to the exotic plant Eupatorium adenophorum Spreng effective ingredient.
US20110021492 Pyridazine derivatives as factor xia inhibitors The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein the variables A, L1, L2, R2, R11, and M are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
US20080139461 Containing the sequence RGD for the preparation of appropriately functionalised antagonists of alpha v beta 3 and alpha v beta 5 integrins; treatment of altered angiogenic phenomena or for the preparation of diagnostically useful compounds The invention relates to novel cyclic peptidomimetic compounds containing the sequence RGD for the preparation of appropriately functionalised antagonists of αvβ3 and αvβ5 integrins, and intended, for example, for the treatment of altered angiogenic phenomena or for the preparation of diagnostically useful compounds.
WO2009097120A1 Methods using immunomodulatory compounds for modulating level of cd59 Provided herein are methods of treating, preventing or managing disorders associated with low CD59 levels. The methods encompass the administration of an immunomodulatory compound provided herein, such as 3-(4-amino-l-oxo-l,3-dihydro- isoindol-2-yl)-piperidine-2,6-dione or 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-4- aminoisoindoline. Further described are methods of treatment using the immunomodulatory compounds in combination with other therapeutic agents or therapies. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.
US20060247260 Bis (hetero) aryl carboxamide derivatives for use as PG12 antagonists This invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) in which Ar1 and Ar2 independently represent phenyl or a 5 or 6-membered heteroaromatic ring, R6 represents carboxyl or tetrazolyl, and the remaining variables are as defined in the text and claims, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension;hemophilia and hemorrhage; and inflammation, since the diseases also relate to PGI2.
WO2009070045A3 Imidazole derivatives, process for their preparation, and thier pharmaceutical use The subject of the present application are derivatives of imidazole, a method of manufacturing them as well as their use as active substance in medicinal products for use in human and veterinary medicine. The derivatives of imidazole according to the present invention are compounds with the general formula (1) in which R1, R2, R3 and n have the meanings as defined in the description.
CN101239069A Application of compound capable of supplying active methyl or engaging in methyl migration The invention relates to the application of a compound which can provide active methyl or participate in methyl transference, in particular to the application of the compound which is used as medicine or health-care food for curing atrophic diseases and delaying senility. The compound which is provided by the invention and can provide active methyl or participate in methyl transference is selected from one or more of elements such as folic acid, vitamin B12, vitamin B6, vitamin B2, sinkaline, lycine, serine and methionine for compounding. The invention also provides a compound for curing atrophic diseases and delaying senility, including at least on compound which can provide active methyl or participate in methyl transference. The compound which can provide active methyl or participate in methyl transference can remarkably reinforce the immunity of the body and the vitality of the cells, can protect the body cells from being damaged by various infectious agents and can cure the atrophic and senile diseases.
US20120022113 Methods for suppressing tipdc trafficking or accumulation and preventing hypercytokinemia The present invention features methods for preventing or ameliorating hypercytokinemia or preventing lethality-associated with infection by highly pathogenic strains of influenza virus by suppressing TNF-α/Inducible nitric oxide synthase-Producing dendritic cell trafficking or accumulation. In particular embodiments, the expression MyD88, CCR2, MCP-I or MCP-3 is targeted.
WO2009067243A8 Modulation of cd40 expression Disclosed herein are antisense compounds and methods for decreasing CD40. Examples of disease conditions that can be ameliorated with the administration of antisense compounds targeted to CD40 include hyperproliferative disorders, graft versus host disease (GVHD), graft rejection, asthma, airway hyperresponsiveness, chronic obstructive pulmonary disease (COPD), multiple sclerosis (MS), systemic lupus erythematosus (SLE), and certain forms of arthritis.
CN102133325A Liniment drug for traumatic injuries The invention discloses a liniment drug for traumatic injuries, which is characterized by comprising the following components in parts by weight: 1 part of Artemisia rupestris L, 1 part of Jiuzi, 1 part of kusnezoff monkshood, 1 part of root of hemsley monkshood, a part of Paris polyphylla, 0.5 part of sappan wood, 0.3 part of camphor wood, 0.5 part of cassia twig, 0.3 part of madder and 0.3 part of trogopterus dung. The components are dried in the sun and then mixed and soaked in wine Chunliang with alcoholic content of 50-60 for more than 30d to obtain a soak solution liniment; and the proportion of the drug to wine is 1:1.8-2.8. The liniment drug has the remarkable effects of diminishing inflammation and swelling, activating blood circulation, stopping bleeding and pain, and healing wounds and is applied to visible and invisible injuries.
EP0888374B1 HIGH AFFINITY NUCLEIC ACID LIGANDS OF THE COMPLEMENT SYSTEM PROTEIN C1q Methods are described for the identification and preparation of high affinity nucleic acid ligands to Complement System Proteins. Methods are described for the identification and preparation of high affinity nucleic acid ligands to Complement System Protein, C1q. Included in the invention are specific RNA ligands to C1q identified by the SELEX method.
US20070173454 Administering an agent that decreases or regulates the blood level, production, function or activity of gonadotropins-leutinizing hormone, follicle stimulating hormone, activin or follistatin; parkinson's disease The present invention relates to a method for slowing, preventing or delaying senescence or treating or preventing a disease associated with senescence by administering a therapeutically effective amount of at least one physiological agent that decreases or regulates the blood level, production, function or activity of LH or FSH, or that decreases or regulates the production or activity of activin, or that increases or regulates the blood level, production, function, or activity of inhibin or follistatin.
WO2008079521A3 Tricyclic heteroaryl compounds useful as inhibitors of janus kinase The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
US6849602 Compositions for alleviating neuropathic pain with prosaposin receptor agonists The invention provides a method of alleviating neuropathic pain in a subject by administering a neuropathic pain alleviating amount of prosaposin receptor agonist to the subject. The invention also provides a method of inhibiting the onset of neuropathic pain in a subject by administering neuropathic pain alleviating amount of prosaposin receptor agonist to the subject. The present invention also provides prosaposin receptor agonists and the use of these agonists for stimulating neurite outgrowth, inhibiting neural cell death, promoting myelination and inhibiting neural demyelination. In addition, there is provided a method of inhibiting sensory or motor neuropathy by contacting neuronal cells with a composition comprising an effective inhibiting amount of prosaposin receptor agonist.
US20050095681 Intracellular modulators of apoptopic cell death pathways A DNA sequence encoding a glucocorticoid-induced leucine-zipper family related protein (GILR), isoforms, fragments or analogs thereof, said GILR, isoforms, fragments or analogs thereof capable of inhibiting apoptosis and stimulating lymphocyte activity, GILR proteins, isoforms, analogs, fragments and derivatives thereof encoded by the aforesaid DNA sequence, their preparation and uses.
CN102885779A Preparation method of 1-deoxynojirimycin sustained-release pellets The invention discloses a preparation method of 1-deoxynojirimycin sustained-release pellets. The preparation method comprises the following steps of 1, uniformly mixing at least one filling agent, at least one binder and at least one lubricant according to a ratio and processing the mixture into smooth round blank pellet cores, 2, preparing mulberry leaf extract and a polymer binder into a mixed solution and coating the mixed solution on outer layers of the smooth round blank pellet cores to obtain quick-release pellets, and 3, dissolving a retardant, a pore-foaming agent and a plasticizer in a coating solvent, and spraying the solution on outer layers of the quick-release pellets to obtain the 1-deoxynojirimycin sustained-release pellets, wherein a weight increasing ratio is in a range of 5 to 25%. The 1-deoxynojirimycin sustained-release pellets obtained by the preparation method can effectively control drugs to release in a certain time, maintains an effective plasma concentration for 24 hours, does not produce burst effects, and greatly improves 1-deoxynojirimycin effects on a human body. The preparation method has simple processes and can be industrialized easily.
CN1891212A Oral preparation and its preparing method The present invention relates to an immunosuppressant preparation and its preparation method. In the concrete, it is an oral preparation, including 2-p-octylphenethyl-2-aminopropanediol hydrochloride as immunosuppressant, inorganic salt and/or other medicinal auxiliary material or carrier.
WO2014083139A1 Novel amorphous form of ticagrelor The present invention refers to a novel amorphous form of ticagrelor, a process for the preparation thereof, pharmaceutical compositions comprising said novel amorphous form of ticagrelor, and to the use of the novel amorphous form of ticagrelor as medicament.
WO2011143148A1 Substituted n-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof The present invention discloses and claims a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula ( Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.
EP1368336B9 Thiophene substituted amine derivatives as glyt-1 inhibitors The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula (I) or a pharmaceutically acceptable salt thereof.
CN103565817A Application of alginate oligosaccharide The invention relates to the field of biological medicines, and discloses application of alginate oligosaccharide. Test results show that the alginate oligosaccharide, directly acting on bacteria, does not inhibit growth effect of the bacteria, but can improve phagocytic ability of human macrophage THP-1 on foreign matters; the alginate oligosaccharide, after induced stimulation on mice macrophage RAW26.47, can improve F-actin expression, and cell form varies from being round to being fusiform, with increase in length-width ratio. GOM, after stimulating THP-1 and RAW264.7 cells, can obviously enhance killing effect on foreign microorganisms. A mouse in vivo experiment also shows that the GOM can remarkably induce increment in the quantity of mouse ascites immune cells and enhance ability of mouse in removing microorganisms in vivo. Therefore, the alginate oligosaccharide has a broad prospect in preparing medicines and healthcare products for promoting macrophage activity.
WO2009103950A1 Fluorinated pyridin-4-0nes Metal chelating compounds of formula (I) are provided: or tautomers thereof or a pharmaceutically acceptable salt of either characterised in that R1 is selected from the group H and C1-6 alkyl R2, R4 and R5 are independently selected from the group H, C1-6 alkyl, Cl, F, -CHF2, CF3, -C(O)CF3, -CH(OH)CF3 and R6 R3 is selected from the group H, C1-6 alkyl and C1-6 acyl R6 is a group -C(O)-N(R7)(R8) R7 is selected from H and C1-6 alkyl and R8 is selected from H, C1-6 alkyl and a group -CH(R9CO)-N(R10XR11 ). R9 and R10 are independently selected from H, C1-6 alkyl and C1-10 aralkyl and R11 is selected from H and C1-6 alkyl, or R10 and R11 together with the nitrogen to which they are bonded form a 3-8 membered heterocyclic ring wherein at least one of R2, R4 and R5 is F. The compounds of the invention have reduced susceptibility to glucuronidation and microsomal oxidation as compared to current clinical compounds of the same class but in preferred forms have lower molecular weight and have blood brain barrier permeability.
EP1551378A4 Epo d + 5-fu/gemcitabine Methods and compositions for treating hyperproliferative diseases using combinations of one or more epothilones and one or more nucleoside analogs. In some embodiments, the combination includes epothilone D and 5-fluorouracil or 5'-deoxy-5-fluoro-N-[(pentyloxy)carbonyl]-cytidine.
CN101591369B N-glycosyl-3-aryl acrylamide derivative, preparation method and medical function thereof The invention relates to the medicinal chemistry field, specifically relates to a N-(1,3,4,6-4-O-acetyl-2-deoxy-beta-D-glucopyranuronosyl(or galactosyl))-3-aryl acrylamide derivative (I), wherein, the definitions of G and Ar are the same as the instruction, the pharmacological experiment proves that the compound of the invention has the function of inhibiting proliferation of the vascular endothelial cell, and can be used for clinical treatment of tumor or chronic inflammation.
WO2013044341A1 Nanoparticulate magnetic material for thermal applications The invention, "nanoparticulate magnetic material for thermal applications", pertains to the field of specific uses or applications of nanostructures formed by individual manipulation of groups of atoms or molecules as discrete magnetic units composed of metals of the lanthanide group, and relates to a nanoparticulate material coated with an organic or inorganic compound, or with a combination thereof, for heating a localised point or a localized zone on an object exposed to an alternating magnetic field. The product consists of a particulate material, optionally including a biocompatible, organic and/or inorganic coating made from an alloy composed of at least one element of the lanthanide group (LA), at least one transition metal (MT) and at least one metalloid (ML), and represented by LA-MT-ML. The described material can be produced by a physical or a chemical process, or by a combination thereof, and has the novel and inventive feature of allowing the alloy to be heated in a controlled manner, alloy that can be produced from a mixture of pure elements, a mixture of alloys or by recycling already industrialised products. The product described in this patent can be used in applications requiring localised heating or localised magnetic features, such as resin or cement hardening, and in medical applications for the treatment of tumours or imaging diagnosis by means of contrast agents.
CN102389423A Medicinal composition containing ibuprofen sodium salt The invention relates to a medicinal composition containing ibuprofen sodium salt, which is prepared by taking ibuprofen sodium salt and other one or a plurality of medicinal components as active ingredients, and combing the active ingredients with pharmaceutically appropriate auxiliary materials. The medicinal composition can be made into oral preparations, including conventional tablets, dispersible tablets, sustained release tablets, capsules, sustained release capsules, soft capsules, particles, dry suspension, suspension and the like, and used for symptomatic treatment of being antipyretic, antiphlogistic, analgesic and anti-allergic, and improving sleeping.
CN101804022A Gel taking 2alpha, 3beta, 12,13-tetrahydroxy-oleanane-28-acid as active component The invention discloses a gel taking 2alpha, 3beta, 12,13-tetrahydroxy-oleanane-28-acid as an active component and also provides a gel composite. The gel composite is characterized by containing the 2alpha, 3beta, 12,13-tetrahydroxy-oleanane-28-acid (I) taken as the active component and one or more auxiliary materials used for gel, wherein the content of the 2alpha, 3beta, 12,13-tetrahydroxy-oleanane-28-acid in the gel composite is 0.01-2%.
US20100273851 Methods of using proteinacious channels to identify pharmaceutical treatments and risks, and treatments resulting therefrom Methods and therapeutic strategies utilizing proteinacious channels in lipid membranes of mammalian cells. The methods entail administering a pharmaceutical to a lipid membrane of a mammalian cell, and then determining the effect of the pharmaceutical on the electrophysiology of at least one proteinacious channel of the lipid membrane, wherein the proteinacious channel is a Kv7 potassium channel and/or a L-type calcium channel of an airway smooth muscle cell (ASMC). The method can be used to identify pharmaceuticals that may be used to treat asthmatic and other bronchospastic conditions that can lead to airway obstruction, or to perform drug screening to assess potential risk of pharmaceuticals.
CN103416535A Selenium-rich spirit-nourishing tea and production method thereof The invention relates to selenium-rich spirit-nourishing tea and a production method thereof. The selenium-rich spirit-nourishing tea is characterized by comprising the following materials by weight: 20 to 30 percent of selenium-rich codonopsis leaf powder, 5 to 15 percent of selenium-rich astragalus extract, 10 to 20 percent of selenium-rich fiveleaf gynostemma herb leaf powder, and 40 to 52 percent of selenium-rich black tea powder. The production method comprises the step of uniformly mixing the codonopsis leaf powder, the fiveleaf gynostemma herb leaf powder, the black tea powder and the astragalus extract according to a proportion, so as to obtain the selenium-rich spirit nourishing tea. The selenium-rich spirit nourishing tea can achieve the purposes of tonifying qi and blood and improving five organs, adopts the four selenium-rich raw materials, can activate the activity of an anti-oxidant enzyme during qi and blood circulation in vivo, performs an anti-oxidant function, promptly remove metabolism garbage, and maintain the normal functions of tissue and organs.
US7544364 reduced tissue accumulation of the glycopeptide antibiotic, reduced nephrotoxicity and reduced histamine release; side effect reduction Disclosed are pharmaceutical compositions containing a cyclodextrin and a therapeutically effective amount of a glycopeptide antibiotic or a salt thereof. Also disclosed are methods of treating a bacterial disease in a mammal by administering such pharmaceutical compositions.
CN101502580B External-use medicament for treating tinea manus and pedis The invention provides an externally applied medicament for treating tinea of hands and feet, consisting of three parts of powders A, electuary B and spray C, and the main ingredients comprise lightyellow sophora root, giant knotweed rhizome, dark plum fruit, salicylic acid, ketoconazole and the like, thereby having the effects of clearing heat, removing toxin, sterilization and anti-inflammation. The medicament is different from the previous simple treatment proposals for treating the tinea of hands and feet, the powers A is firstly used for rapidly killing pathogens at the skin surface, changing the infected lesion skin tissue structure of the surface, leading the structure to be loose and forming a smooth channel which is conductive to the penetration of the medicament, then the electuary B is used under the premise of the channel for dredging the penetration of the medicament, thereby rapidly and thoroughly killing the pathogens in skin, the spray C is used for powerful sterilization, keeping a clean environment for the skin and achieving the effect of no recurrence. The medicament carries out multi-level three-dimensional treatment, simultaneously realizes the treatment of external and internal diseases, combines the prevention with the treatment and simultaneously treats both principal and secondary aspect of disease, thereby realizing the special treatment method and reliable efficacy.
CN101756979A Fexofenadine hydrochloride orally disintegrating tablet and preparation method thereof The invention provides a preparation method of fexofenadine hydrochloride orally disintegrating tablets. Based on the advantages of the orally disintegrating tablet preparation formulation, the product not only overcomes the defects of poor disintegration, slow effect, low bioavailability and the like of the preparation formulations on sale in foreign countries, but also fills a gap in the domestic market, thus adapting to the demand of development of market situation. The medicine has important significance in keeping good health of the people and creating economical and social benefits. The product has simple and easy technique and easily obtained raw and auxiliary materials, is suitable for industrial production, and has good application prospect.
CN101006993A Soluble slow release external applied contraceptive The invention discloses an externally-applied soluble slow release contraceptive, which comprises nonoxynol 1.2-2.0 parts, chitosan 10-20 parts, humectant 5-20 parts and water 200-500 parts. The medicament can be released continuously.
CN1733314A Process for preparing cerebrose albumin magnetic adriamycin nanometer particle Disclosed is a process for preparing cerebrose albumin magnetic adriamycin nanometer particle, which comprises preparing cotton seeds oil, nano magnetisable powder and galactose albumins, mixing Azithromycin, galactose albumins and magnetisable powder by a predetermined proportion, carrying out ultrasonic emulsifying in refined cotton seeds oil, heating, solidifying and ether washing.
WO2007020935A1 Therapeutic agent for pain comprising p2y12 receptor and/or p2y14 receptor blocker [PROBLEMS] To provide a therapeutic agent for pain. [MEANS FOR SOLVING PROBLEMS] A preventive agent, a therapeutic agent and/or an agent for inhibiting symptom development for pain comprising a P2Y12 receptor and/or P2Y14 receptor blocker. By administering the P2Y12 receptor and/or P2Y14 receptor blocker, pain, particularly neuropathic pain, for example, cancer pain, postherpetic pain, diabetic pain, HIV related neuropathic pain, pain caused by stone, neuralgia, orofacial pain or pain in disease such as hyperalgesia can be significantly improved.
EP2334656A1 Triazole compounds, use thereof, and agents containing same The invention relates to compounds of formula (I) wherein the variables have the designations defined in the claims and in the description, and to the use thereof as fungicides or in an antimycotic agent.
US20080096897 water soluble; lower toxicity by photosensitization; anticancer; antitumor; antiinflammatory; arthritis; osteoporosis; ocular abnormal angiogenesis; multiple sclerosis, asthma, atherosclerosis New Pyrimidinetrione derivatives represented by formula (I), wherein R1 and R2 are defined in the description, composition thereof, and methods of preparation are described. The compounds are useful in the treatment of disease involving metalloproteinases.
US20080066744 Process for producing metered dose inhaler formulations Disclosed are methods of introducing a suspension or solution of a medicament, preferably mometasone furoate anhydrous, into a metered dose inhaler container, said container having a valve attached thereto, said method comprising the steps of introducing mometasone furoate anhydrous, a surfactant and a chlorofluorocarbon free propellant into a vessel that is held under pressure to form a suspension or solution, circulating said suspension or solution from the vessel through a line which includes a filling head, bringing said filling head into communication with said metered dose inhaler container through said valve of said metered dose inhaler container, introducing a quantity of such suspension or solution into the container from the filling head of the line through said valve of said metered dose inhaler container, withdrawing said filling head from said metered dose inhaler container, and sealing said metered dose inhaler container, as well as the products produced thereby having an improved particle size distribution of the active ingredients in metered dose inhalers.
WO2011079016A1 Methods of treating hbv and hcv infection This application relates to a purine derivative and pharmaceutical compositions which are useful for treating a hepatitis B viral infection or a hepatitis C viral infection.
EP2740481A1 Method for filling bone cavity formations with calcium The invention proposed is a method for filling bone cavities in metaphyseal (trabecular) bone sections and prevention of calcium secretion, from bones. The proposed method lies in supply of drone brood in combination with calcium administration. The existing methods of body saturation with calcium do not provide the desired effect.
CN102935094A Composite for diabetes The invention discloses a composite for diabetes. The composite comprises substances of propolis, chromium yeasts and vitamin E. Compared with the prior art, the composite mainly uses the propolis, and the vitamin E is added in the propolis, so that the auxiliary blood sugar decreasing effect of the propolis can be enhanced; the combined usage of the vitamin E and chromium can regulate the sugar metabolic level of diabetes, and pancreatic beta cells are protected. Accordingly, the combined usage of the propolis, the chromium and the vitamin E has an obvious blood sugar decreasing effect. The three materials have no incompatibility, and combined usage has a good auxiliary blood sugar decreasing effect.
US20090038024 Cap/sorbs1 and diabetes The present invention provides methods, compositions, and kits useful for modulating insulin/glucose homeostasis in a subject by modulating CAP/SORBS1. In addition, the invention provides a variety of prescreening and screening methods aimed at identifying agents that modulate insulin/glucose homeostasis. Methods of the invention can involve assaying test agent binding to CAP/SORBS1 polypeptides or polynucleotides. Alternatively, test agents can be screened for their ability to alter the level of CAP/SORBS1 polypeptides, polynucleotides, or action.
EP1649856A2 Use of pimecrolimus for selective immunomodulation The invention relates to methods to produce selective immunomodulation in epithelial tissues to treat epithelial inflammatory disorders. This invention provides methods for the use of pimecrolimus to treat epithelial inflammatory disorders including asthma and inflammatory bowel disease while minimizing systemic side effects.
US7402696 exert an ACC activity-inhibiting effect that is effective in the treatment of obesity, hyperlipemia, fatty liver, hyperglycemia, impaired glucose tolerance, diabetes, diabetic complications (diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, and diabetic macroangiopathy, hyperten The present invention provides novel benzene compounds presented by the following formulas, and analogs thereof, that exert an ACC activity-inhibiting effect that is effective in the treatment of obesity, hyperlipemia, fatty liver, hyperglycemia, impaired glucose tolerance, diabetes, diabetic complications (diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, and diabetic macroangiopathy, hypertension, arteriosclerosis), hypertension, and arteriosclerosis.
US20070280924 Pharmaceutical Preparations For And Treatment Of Ocular Surface and Other Disorders A pharmaceutical preparation suitable for use in the eye, which comprises: (i) a pharmaceutically acceptable carrier suitable for use in the eye; (ii) one or more ingredients selected from factors and agents that promote any one or more of survival, health, cell attachment and normal differentiation of ocular surface epithelial cells and optionally factors and agents to prevent squamous metaplasia; (iii) one or more agents capable of altering the fluid properties of a tear film including at least one agent capable of establishing and/or maintaining a stable tear film and optionally one or more agents selected from opthalmological lubricating agents, viscosity enhancing agents and agents capable of reducing tear film evaporation; the factors and agents in component (ii) and (iii) being synthetic or recombinant or licensed for pharmaceutical use.
US7645763 dipeptidylpeptidase-IV inhibitors; antidiabetic agents, antiarthritic agents, obesity, allograft transplantation, and osteoporosis caused by calcitonin; 1,3-disubstituted-7-(2-butyn-1-yl)-8-(3-aminopiperidin-1-yl)-xanthine compounds The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, the tautomers, the stereoisomers, the mixtures thereof, and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
WO2009128919A1 Deuterium bearing analogs of anastrozole as aromatase inhibitors for the treatment of breast cancer This invention relates to novel, substituted aralkyl heterocyclic compounds according to formula I, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering aromatase inhibitors. Formula (I), or a pharmaceutically acceptable salt thereof, wherein: each R1 is independently selected from CH3, CH2D, CHD2 or CD3; each R2 is independently selected from CH3, CH2D, CHD2 or CD3; each Y is independently selected from H or D; and when each R variable is CH3, at least one Y is D.
US7842699 administering 3-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile or salts, for the treatment of dermatitis, Crohn's disease, inflammatory bowel disease, transplant rejection, lupus, multiple sclerosis, arthritis, psoriasis, diabetes and autoimmune diseases A compound of the formula wherein R1, R2 and R3 are as defined above, which are inhibitors of the enzyme protein kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, xeno transplation, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.
CN102145181B siRNA for inhibiting tumor growth and oligomeric nucleic acid combination and application of siRNA The invention discloses a siRNA for inhibiting tumor growth and oligomeric nucleic acid combination and application of the siRNA. The oligomeric nucleic acid of the invention is double-strand RNA as the following 1) or 2): 1) oligomeric nucleic acid siPTN consisting of sequence 1 and sequence 2 in a sequence table; and 2) double oligomeric nucleic acid consisting of the oligomeric nucleic acid siPTN of 1) and miR-34a, wherein the miR-34a is the oligomeric nucleic acid consisting of sequence 3 and sequence 4 in the sequence table. Tumor cells are inoculated to nude mice, and after tumors are formed, the experiment in which the oligomeric nucleic acid is used for treatment proves that the oligomeric nucleic acid combination can inhibit in-vivo growth of tumors effectively. As a novel small nucleic acid-type antitumor drug, the siRNA chemically synthesized and modified is hardly degraded, has long effect half-life, and can be used for in vitro experiment, even for in vivo treatment.
EP1932843A1 Sulfonyl-phenyl-2H-(1,2,4) oxadiazole-5-one derivatives, processes for their preparation and their use as pharmaceuticals The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
CA2814846A1 Cyclic amine substituted oxazolidinone cetp inhibitor CCompounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, A3 is a substitiuted phenyl group or indanyl group.Formula (I).
CN102488812A Bone fracture oral medicine, preparation method thereof, and application method thereof The invention relates to a formula of an oral medicine used for treating bone fracture, a preparation method thereof, and an application method thereof. The medicine is composed of medicine materials of, by weight: 10-15 parts of ligusticum, 10-15 parts of yanhusuo tuber, 10-15 parts of white peony root, 10-15 parts of safflower, 10-15 parts of angelica archang lica, 10-15 parts of dipsacus asper, 10-15 parts of ground beetle, 10-15 parts of fortune's drynaria rhizome, 10-15 parts of native copper, 10-15 parts of dragon's blood, 10-15 parts of suberect spatholobus stem, 10-15 parts of eucommia, 10-15 parts of prepared rehmannia rhizome, 10-15 parts of licorice root, and 10-15 parts of radix notoginseng powder. The medicine materials can be prepared into decoctions or pills. According to different phases of the pathogenetic condition of a bone fracture patient, such as an early-stage, a middle-stage or a later-stage, treatments are carried out by using different preparation forms. With the medicine provided by the invention, bone fracture can be rapidly cured with an effective rate of 100%. The medicine application is flexible, and a targeting effect is good. The medicine can be effectively delivered to a bone fracture position, such that the effect of the medicine can be better developed. The oral medicine causes no toxic or side effect.
WO2012070621A1 Use of age-specific aptamer for treating renal disease The present invention provides a composition for treating or preventing diabetic renal disease, and the composition comprises an AGE-binding aptamer as an active ingredient.
CN101301260A Sustained-release agent containing carbenicillin and use thereof A sustained release preparation containing carbenicillin consists of sustained release microsphere and dissolvant, wherein the sustained release microsphere contains sustained release auxiliary materials and penicillins antibiotic; the dissolvant is special dissolvant containing suspending agents such as sodium carboxymethyl cellulose, and the viscosity of the dissolvant is 100 to 3,000 cp (at a temperature of between 20 and 20 DEG C); the sustained release auxiliary materials are selected from EVAc, Polifeprosan, PLA, PLGA, sebacic acid copolymer, albumin glue and gelatin, etc.; the sustained release microsphere can also be made into a sustained release implantation agent. The sustained release implantation agent and sustained release injection can be partly placed or injected into a bacteria focus so as to slowly release medicine over local bacteria focus for 5 to more than 30 days, thereby obviously reducing whole-length toxicity while effectively obtaining and maintaining the effective drug concentration of local focus. The sustained release preparation has remarkable and unique therapeutic effects in curing infections caused by staphylococcus, streptococcus, peptostreptococcus, propionibacterium acnes, enterobacter, tubercle bacillus, gonococcus or meningococcus, etc., and local focuses in particular such as chronic osteomyelitis, severe bedsore, intractable skin ulcer, diabetic foot, femoral head necrosis and various abscesses.
WO2011057169A3 Improved silver oxide formulations A formulation including at least one silver oxide including a silver(II) oxide, the silver(II) oxide having an irregular macrocrystal structure, the silver oxide having an average particle size (D50) below 8 micrometers, the irregular macrocrystal structure characterized by a diffraction peak in a {111} diffraction plane having at least one of the following structural properties: (i) a measured full width half maximum (FWHM) of the peak being at least 0.24 degrees of 2θ; and (ii) a net full width half maximum (net FWHM) of the peak being at least 0.14 degrees of 2θ.
CN101199470A Calcite medical dental cream and process for preparing same The invention provides a gypsum rubrum medical toothpaste. The toothpaste is made with processed calcite as the main active medical material and commonly used toothpaste base material through common technique. The gypsum rubrum medical toothpaste integrates the functions of diminishing inflammation, stopping bleeding, easing pain and detumescence and has good effects in curing gingival bleeding and teethridge abscess and can care the mouth well and keep the foul breath fresh.
EP0515460B2 Docosahexaenoic acid, methods for its production and compounds containing the same This invention relates to a process for producing a single cell edible oil containing DHA, Docosahexaenoic acid, to the oil itself and to uses for the oil. A marine microorganism, such as Crypthecodinium cohnii, is cultivated in fermentors and induced to produce the single cell oil which subsequently is recovered by extraction with solvents.
EP1334721B1 Nateglinide-containing hydrophilic drug preparations Hydrophilic drug preparations containing nateglinide B crystals useful as a hypoglycemic agent as the active ingredient which comprise a hydrophilic substance selected from the group consisting of hydrophilic polymers, surfactants, sugars, sugar alcohols and salts, and thus have a contact angle of the preparation surface to water of 111 DEG or less. These preparations, which are quick release preparations having high elution properties, can be easily produced.
WO2012089137A1 Arylurea compound, intermediate and use thereof Disclosed in the present invention is an arylurea compound represented by formula I, or a pharmaceutically acceptable salt, a polymorph, a solvate or a stereoisomer thereof, and an intermediate and use thereof. The arylurea compound I of the present invention has protein kinase inhibiting activity, and antitumor and anti-angiogenesis activity.
CN1927210A Sterilization film coating agent for burn and scald wound The invention relates to a sterilization type film coating agent for the treatment of burns and scalds, wherein the main constituents include white Vaseline, cellulose glycollic ether, silver sulfadiazine, Tween-80, distilled water and highly effective germicidal agent.
US20120270826 Adult stem cells, molecular signatures, and applications in the evaluation, diagnosis, and therapy of mammalian conditions The present invention relates to the identification of a stem cell-specific signature or signatures composed of protein and/or nucleic acid markers expressed by virtue of the position of a cell or cells in the time line of its/their development and the impact of the cells' environment on this signature as it relates to the cells' stem cell potential. The composition and combination of these signatures provides a means of identifying, manipulating and differentiating said adult stem cells and thus, their acquisition and utilization in research, diagnosis, and therapy of normal and pathological conditions.
WO2013023622A1 Acylated derivative of homoharringtonine, preparation method therefor, and application thereof The present invention relates to the fields of natural medicine and medicinal chemistry, and relates to, as represented by Formula (I) and Formula (II), a novel acylated derivative of homoharringtonine or a pharmaceutically acceptable salt thereof, a method for preparing said compounds, a pharmaceutical composition comprising the compound, and an application thereof in preparing an antitumor medicament.
CN103108556A Ingredients derived from sphaeranthus indicus The invention discloses herbal ingredients derived from Sphaeranthus indicus standardized to at least one frullanolide/eudesmanoid sesquiterpene compound and their compositions as natural energy enhancer to provide an onset and steady maintenance of energy and mental alertness in a mammal. The invention further includes the use of ingredients and compositions for food ingredient formulations such as dietary supplement, food ingredient, beverage, snack or energy drink containing the above said herbal ingredient(s) for enhancing physical activity, physical fitness, mental alertness, enhancing energy levels, stamina levels, circulatory health, blood vessel health and for better mental health in warm blooded animal.
WO2007009705A1 (rac)-n-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydr0-1h-pyrazole-3-carboxamide hydrates The present invention relates to (rac)-N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H- pyrazole-3-carboxamide • X H2O, with X between 0.7 and 0.3. Especially preferred is (rac)-N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H- pyrazole-3-carboxamide • monohydrate. Methods for their preparation, and their use as modulators of the cannabinoid receptor are also disclosed.
US20090012173 Method for treatment of nocturia A method for treatment of nocturia by administering to a mammal, such as a human, in need of such treatment, a therapeutically effective amount of loxoprofen or a pharmacologically acceptable salt thereof.
CN101613334B Flavonoid derivative and medical application thereof The invention relates to a flavonoid derivative of which an oxygen atom is substituted by alkyl-carboxylic acid or pharmaceutically acceptable salt thereof, a medicine composition containing the compounds as active components and an application of the flavonoid derivative or the pharmaceutically acceptable salt of the flavonoid derivative for preparing a lipid-lowering medicine.
WO2014020160A1 Article of manufacture comprising aflibercept or ziv-aflibercept Article of manufacture comprising a packaging material, a polypeptide of SEQ ID NO:1, aflibercept or ziv-afliberceptor a biosimilar thereof, and a label comprising a printed statement which informs a prospective user of adverse events or adverse reactions.
CN101147738A Dihydroartemisinin and metronidazole combination The present invention relates to a medicine composition formed from dihydroartemisinin and metronidazole and its application for preventing and curing trichomonas vaginalis.
CN101863926A Antitumor drug palladium coordination compound The invention belongs to the field of pharmacy and relates to an antitumor drug palladium coordination compound. The palladium coordination compound has the structural formula shown in the specification, and in the formula, a ligand L is selected from aliphatic diamine or substituted aliphatic diamine, aromatic diamine and various substituted aromatic diamine, and R1 and R2 are respectively selected from substituted or unsubstituted branch, linear chain or annular aliphatic hydrocarbon, aryl group, non-aromatic family or aromatic heterocyclic groups.
CN102643225A Ionic liquid, nano fluorescent ellipsoid and preparation method thereof The invention relates to ionic liquid, a nano fluorescent ellipsoid and a preparation method thereof, belonging to the field of ionic liquid. The ionic liquid reacts with fluorescent silicon dioxide nano spheres with amino on surface at room temperature and is connected onto the nano spheres through C=N double bonds. Besides, under the nonbonding effect (self-assembly) of groups, brominated 4-acetylpyridyl which is connected onto the surfaces of the nano spheres form a novel ionic liquid modified nano ellipsoid. The diameter of the nano ellipsoid is 200-210nm. The nano ellipsoids can be selectively adsorbed on the surfaces of tumor cells to improve tumor fluorescence imaging. The nano ellipsoids can induce the death of the tumor cells and the half maximal inhibitory concentration is 15mg ml<-1>. The novel carbonyl functionalized ionic liquid which is used for nano ellipsoid preparation, tumor fluorescence imaging and anti-tumor activity researches is reported for the first time in the world and can be used for tumor diagnosis and fluorescence detection and treatment.
CN103349662A Application of Myriberine A in anti-depression drug preparation The present invention relates to an application of Myriberine A in anti-depression drugs, and provides a use of the Myriberine A in anti-depression drugs, wherein the Myriberine A can be adopted as a drug for prevention or treatment of depression. According to the present invention, the use of the Myriberine A in anti-depression drug preparation is firstly disclosed, the skeleton belongs to a completely-new skeleton type, anti-depression activity of the drug is strong, possibility that any revelation is provided by other compounds does not exist, the drug has prominent substantive characteristics, and significant progress is provided for anti-depression drugs.
WO2006034463A3 Herbal supplement to support weight loss Disclosed herein are herbal and chemical combinations for promoting weight loss. The herbs in the composition can include, among others, green tea, ginger, cocoa, and yerba mate. Other chemicals in the composition can include, among others, caffeine and a pharmaceutically acceptable salt of calcium.
US7109174 Anticonvulsant derivatives useful for preventing the development of type II diabetes mellitus and syndrome X Anticonvulsant derivatives useful for preventing the development of Type II diabetes mellitus and Syndrome X are disclosed.
WO2005123711A1 Bicyclol glycosides and the preparation method and uses thereof The present invention relates to pharmaceutics and organic chemistry. The invention discloses a new kind of bicyclol glycosides and the preparation method thereof. The method comprises bicyclol being reacted with trichloroimide ester of acylating sugar in the presence of a conventional solvent to carry out glycosidation, and the acylated glycosides being treated with sodium alkoxide to form the bicyclol glycosides. The present bicyclol glycosides is useful for the treatment of hepatopathy.
EP1686979A2 Activation of hypoxia-inducible gene expression The present invention relates to the elucidation of specific molecular features of endogenous 2-oxoacid molecules and their derivatives for activating hypoxia-inducible e gene expression by inactivating hypoxia-inducible factor hydroxylating enzymes. This invention identifies agents that can be used to induce tissue vascularization, treat anemias, induce tolerance to stroke and heart attacks, improve tissue healing and improve organ transplantation.
CN103214429A 1-substituted phenyl-3-(N-phenothiazinyl)propyl-2-ene-1-ketone as well as preparation method and application thereof The invention relates to 1-substituted phenyl-3-(N-phenothiazinyl)propyl-2-ene-1-ketone as well as a preparation method and an application thereof. The structural formula of 1-substituted phenyl-3-(N-phenothiazinyl)propyl-2-ene-1-ketone is shown in the specification, wherein R is 4'-F, 4'-Cl, 4'-Br, 4'-CH3, 4'-NO2, 4'-OCH3 or 3'-NO2. The preparation method comprises the following steps of placing N-formyl phenothiazine and substituted acetophenone in a reaction vessel, the placing sodium hydroxide or potassium hydroxide into the reaction vessel, grinding, monitoring the reaction by utilizing thin layer chromatography (TLC), stopping the grinding when a raw material point of reactants disappears, adding water into the reaction vessel to wash products, filtering the turbid liquid in vacuum after washing the products, and washing and vacuum-drying the filter cake to obtain 1-substituted phenyl-3-(N-phenothiazinyl)propyl-2-ene-1-ketone. The grinding method is used for facilitating the reaction of raw materials, so that the step is simple, the raw materials are easy to obtain, the reaction time is short, and the after-treatment is simple; and the product is high in yield and purity, has an antibacterial activity, and can be applied to the field of biological medicines.
US7589189 By using a double-stranded RNA (dsRNA); neurodegenerative disorder It is intended to provide methods for suppressing the huntington gene expression by using a double-stranded RNA (dsRNA), huntington gene expression inhibitors to suppress the huntington gene expression, and preventives and/or remedies of Huntington's disease. Targeting against a specific sequence of mRNA at immediately upstream of CAG repeats in HD genes of Huntington's disease, the huntington gene expression is suppressed by using a dsRNA homologous to the sequence. In this invention, a short siRNA (short double-stranded RNA) having bp as short as around 21-23 bp can be effectively used as the dsRNA homologous to a specific RNA sequence in a region at immediately upstream of CAG repeats. The dsRNA of this present invention can be used as a huntington gene expression inhibitor, or a preventive and/or a remedy of Huntington's disease by administering or introducing into a living body or a living cell in mammals for the prevention and/or treatment of Huntington's disease.
CN102988683A Kidney and spleen tonifying pill for preventing and treating osteoporosis The invention provides a kidney and spleen tonifying pill for preventing and treating osteoporosis. The pill is prepared by uniformly mixing, crushing and pelleting the following components in parts by weight: 8 to 15 parts of astragalus, 8 to 12 parts codonopsis pilosula, 8 to 12 parts of fried bighead atractylodes rhizome, 8 to 12 parts of fried yam, and 30 to 60 parts of chondroitin sulfate. The product has good effect of preventing and treating osteoporosis.
US7659115 Nucleic acid encoding human transductin-1 polypeptide The invention provides isolated or purified nucleic molecules consisting of a nucleotide sequence encoding human transductin-1 (TDC1), such as SEQ ID NO: 1. The invention also provides vectors comprising the isolated or purified nucleic acid sequences and cells comprising such vectors.
EP2163246A1 Taurine or taurine-like substances for the prevention of the irreversible visual effects of vigabatrin The present invention relates to taurine or taurine-like substances for the prevention of the irreversible visual effects of vigabatrin. More particularly the invention relates to a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis for the prevention of the irreversible visual effects of vigabatrin.
US20090202439 Methods for treatment of angiogenesis The present invention includes methods for treatment and prophylaxis of diseases, post-surgical disorders and bacterial infections associated with lactosylceramide. The methods generally provide for administration to a subject one or more compounds that alter the activity of VEGF pathway members, including LacCer synthase (GalT-V/VI), PECAM1, VEGFR, VEGF or related pathway members to treat a subject suffering from or susceptible to a condition caused or contributed to by VEGF. The present invention also relates to methods for detecting and analyzing compounds with therapeutic capacity to treat such condition.
US20120232121 Use of sarcoplasmic ca2+-atpase type 2 protein for diagnosing and treating learning or mental disorders The present invention embraces methods for the diagnosis and treatment of learning or mental disorders, as well as the identification of agents useful in the treatment of such disorders based upon the identified involvement of Sarcoplasmic Ca2+-ATPase type 2 Protein in synaptic plasticity and neurotransmitter release in 22q11 deletion/DiGeorge Syndrome.
CN101230082B 23-hydroxy betulinic acid derivative, preparation method, preparation and use thereof The invention relates to modified 23-hydroxybetulinic acid derivative (1), which belongs to the natural medicine and pharmaceutical chemistry field. The definition of R1, R2, and R3 is shown in the instruction. The invention also discloses a preparation method of the 23-hydroxybetulinic acid derivative, the medicine composition containing the 23-hydroxybetulinic acid derivative, and the use thereof in tumor resistance.
CN101050213A Fat amido substitutional berberine derviation, preparation method, and application of anticancer drugs This invention discloses a method for preparing 9-fatty-amino-substituted berberine derivative used as an anti-tumor agent. A fatty-amino side chain is introduced to 9-site of berberine frame. The berberine derivative can react with telomere DNA or proto-oncogene c-myc DNA, and inhibit the activities of telomere/telomerase in tumor cells and expression of proto-oncogene c-myc DNA. Experiments show that the berberine derivative can inhibit several tumor cell lines, and has low toxicity on normal cells. The berberine derivative can thus be used to prepare anti-tumor drugs.
WO2005027968A1 Remedy for down syndrome It is intended to provide a remedy and a therapeutic method for Down syndrome, which cannot be fundamentally treated, aiming at ameliorating congenital mental and motile developmental disorders and improving daily behaviors and socialization to thereby finally achieve participation of patients in society. Namely, a remedy for Down syndrome, an agent for ameliorating mental developmental disorders in Down syndrome or an agent for improving daily behaviors each comprising an acetylcholine esterase inhibitor. More specifically speaking, the acetylcholine esterase inhibitor is donepezil hydrochloride. Still specifically speaking, a remedy for Down syndrome, an agent for ameliorating mental developmental disorders in Down syndrome or an agent for improving daily behaviors for patients with Down syndrome who have intelligent quotient values of 48 or lower and/or patients with Down syndrome who are 36 years old or younger.
CN103525639A Pyrroloquinoline quinone-containing wine The invention provides a pyrroloquinoline quinone-containing wine. The wine comprises the following components in percentage: 0.01-10 percent of pyrroloquinoline quinone, 0.01-1 percent of stabilizer, 0.01-1 percent of cosolvent and 88-99.9 percent of wine. The pyrroloquinoline quinone-containing wine can specifically prevent alcoholic fatty liver and inhibit the process of diseases and has a good market prospect.
US20110313010 Combination of local temozolomide with local bcnu The additive effect of combined intracranial carmustine (“BCNU”) with intracranial temozolomide (“TMZ”), and particularly in combination with radiation (“XRT”), in the treatment of two rat intracranial glioma models, the 9L gliosarcoma and the F98 glioma, demonstrates that local delivery of both drugs, especially in combination with radiation, is far more effective than delivery of either drug alone or one systemically and one locally, either with or without radiation. The triple therapy showed a significant improvement in survival when compared to controls (p=0.0004), local BCNU (p=0.0043), oral TMZ (p=0.0026), local TMZ (p=0.0105), and the combinations of either BCNU and XRT (p=0.0378) or oral TMZ and local BCNU (p=0.0154).
WO2009074320A1 Method for odor extinction The invention relates to the use of a pharmaceutically acceptable reduction agent having a reactive thiol group for organic compounds containing disulfide bridges for the treatment of odor formation in a human due to the ingestion of garlic plants, or parts thereof.
CN103070945A Ephedra forsythia tablet The invention relates to an ephedra forsythia tablet. The ephedra forsythia tablet is mainly composed of following drugs: ephedra, almond, plaster, honeysuckle, forsythia and prepared liquorice root.
WO2007059905A2 Thienopyrimidines treating inflammatory diseases The present invention relates to the use of thienopyrimidine compounds for the production of pharmaceutical compositions for the treatment of inflammatory diseases.
EP1385499B1 Use of carnitine for the preparation of an injection solution for preventing or alleviating ascites in poultry by in-ovo injection Carnitine is injected in-ovo in incubating eggs of poultry in order to improve the well-being of poultry and/or prevent or alleviate ascites. A small amount of carnitine injected in ovo shows an efficacy similar to conventional feeding techniques requiring larger amounts of carnitine.
EP2045248A1 Method for preventing coloration of catechins and dentifrice composition The present invention relates to a method of suppressing coloration of catechins, which contains adding, to catechins, a water-soluble polymer forming a water-insoluble complex with catechins, as well as hydrogel particles containing a water-insoluble complex between catechins and a polymer forming a water-insoluble complex with catechins. Further, the present invention relates to a dentifrice composition containing hydrogel particles containing catechins and a polymer forming a water-insoluble complex with catechins, a binder and water.
WO2014164780A1 Fused tetracyclic bromodomain inhibitors The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Y2, A1, A2, A3, and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
CN103524421A Novel naphthoyl urea derivate and medical application thereof The invention relates to a novel naphthoyl urea derivate. The substance can obviously restrain VEGFR2 and PDGFR-beta receptor tyrosine kinase from phosphorylation in a nanomole concentration level, and as a novel tyrosine kinase inhibitor, the novel naphthoyl urea derivate can be applied to treatment of diseases or symptoms, such as cancer, mediated by tyrosine kinase as well as ophthalmic diseases together with new pathologic vessels.
US8592422 Bicyclic triazole and pyrazole lactams as allosteric modulators of mGluR5 receptors In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
CN103751794A Vitamin E-containing cyclodextrin clathrate The invention provides a vitamin E-containing cyclodextrin clathrate. The vitamin E-containing cyclodextrin clathrate comprises vitamin E and hydroxypropyl-beta-cyclodextrin. The hydroxypropyl-beta cyclodextrin coats vitamin E so that the vitamin E-containing cyclodextrin clathrate is obtained. A weight ratio of vitamin E to hydroxypropyl-beta-cyclodextrin is in a range of 10-20%. The vitamin E-containing cyclodextrin clathrate further comprises povidone K29/32. The amount of povidone K29/32 is 10-50wt% of that of hydroxypropyl-beta-cyclodextrin. The vitamin E-containing cyclodextrin clathrate can be processed to form tablets, capsules, powder or a powder injection.
US7094895 Inotropic agents such as (S)-N-tert-butyloxycarbonyl-N-methyl-tyrosyl)-4-(4-nitrophenyl)-piperazine, used for preventing and/or prophylaxis of diseases associated with adenosine 5'-triphosphate The present invention relates to compounds of the formula wherein R1 and R2 are independently hydrogen, C1–C4 alkyl, C1–C4 substituted alkyl, C1–C4 alkoxy, C1–C4 substituted alkoxy, C1–C4 acyl, halogen, cyano, nitro, amino, alkylamino, or dialkylamino; R3, R4, R5, R6, R7, and R8 are independently CH or nitrogen; R9 is hydrogen or methyl; R10 is C═O or (CH2)n; where n is 0, 1, 2, 3, or 4; R11 and R12 are independently nitrogen or CH; X1 and X2 are independently hydrogen, deuterium, tritium or halogen; and X3 is N; and their pharmaceutically acceptable salts; compositions thereof. Methods of preparing the compounds are also described. The compounds are useful in the treatment of diseases in mammals that are mediated by the action of the P2X7 receptor.
US7064190 An isolated complex of a peptide of glutamic acid decarboxylase(with specific 6 contiguous amino acids), and an allele of MHC class II molecules DR3 and DR4; useful for diagnosis and therapy of autoimmune diseases The invention concerns autoreactive peptides, peptide-MHC complexes, T cell subpopulations that react thereto as well as diagnostic and therapeutic applications of these compounds.
CN1957971A Health products for decreasing blood fat A hypolipemic health-care food for decreasing blood fat, blood sugar, and blood pressure, improving immunity, dissolving thrombus and resisting against virus and tumor is proportionally prepared from natto powder, lentinan, kakonein, and theapolyphenol through mixing.
CN101810617A Preparation method and quality test method of pseudoephedrine hydrochloride and dextromethorphan hydrobromide chewable tablets The invention discloses a preparation method and a quality test method of pseudoephedrine hydrochloride and dextromethorphan hydrobromide chewable tablets. The preparation method is characterized in that: medicaments are dispersed in sodium alga acid uniformly first; then auxiliary materials are added, and the mixture is granulated; and finally, the grains are coated with a coating material to isolate the bitterness of medicaments. The quality test method comprises thin layer chromatography and a content measurement method, has high specificity and ensures the preparation process of the invention has high controllability.
EP1304371B1 Cds1 knockout mice and cell lines established thereof ES cells having been inactivated in one of the loci are established by using the gene targeting method. Then a chimeric mouse is constructed by using the above cells and a genetically modified mouse having been inactivated in both of the Cds1(Chk2) gene pair is thus constructed. The ES cells having been inactivated in one of the gene pair are incubated in a selection medium at a higher concentration to give a mouse ES cell line having been inactivated in the other one of the gene pair too. This mouse or the cells established form this mouse are usable in screening a compound which controls the cell cycle.
CN102872433A Nourishing pill The invention discloses a nourishing pill, which comprises the following raw materials in parts by weight: 5 to 8 parts of rhizoma dioscoreae, 5 to 8 parts of fructus lycii, 2 to 4 parts of dried ginger, 6 to 8 parts of radix angelicae sinensis, 0.1 to 0.3 parts of cinnabar, 1 to 4 parts of radix asparagi, 0.2 to 0.6 parts of manis pentadactyla, 1 to 3 parts of wild chrysanthemum, 2 to 6 parts of sucrose and 1 to 2 parts of essence. The nourishing pill provided by the invention has the effects on tonifying the spleen and nourishing the stomach, promoting production of body fluid and nourishing the lung and tonifying kidney and arresting seminal emission.
US20090209576 Pharmaceutical composition containing clopidogrel camphorsulfonate or polymorphic forms thereof A pharmaceutical composition of the present invention which comprises clopidogrel camphorsulfonate of formula (I) or its polymorphic forms as an active ingredient is useful for treating or preventing a platelet aggregation-associated disease.
CN101569654B Application of pigeon pea stilbene acid in the preparation of antitumor drug The invention relates to a supercritical extract of pigeon pea leaves and the new application of the main component of the extract ---pigeon pea stilbene acid (containing pigeon pea stilbene acids I-VI) in antitumor aspect. After different excipients are added to the pigeon pea stilbene acid, the pigeon pea stilbene acid can be processed into any pharmaceutical dosage form. The supercritical extract of pigeon pea leaves and pigeon pea stilbene acid (containing pigeon pea stilbene acid I-VI) has the characteristics of light toxic and side effect, accurate curative effect, safety, reliability, and the like. Pigeon peas have the advantages of abundant resources, convenient collection, simple extraction process and convenience for industrial production.
WO2012097223A2 Oligosaccharide conjugates for targeting bacteria and uses related thereto This disclosure relates to conjugates for targeting bacteria and related uses. In certain embodiments, the disclosure relates to methods of transferring a molecule of interest into bacteria comprising mixing bacteria with a non-naturally occurring conjugate under conditions such that the conjugate is transported across the bacterial cell wall. Typically, the conjugate comprises an oligosaccharide and a molecule of interest. In certain embodiments, the molecule of interest may be a tracer or an antibiotic.
US8668934 Pharmaceutical formulation comprising a water-insoluble active agent A method of preparing a pharmaceutical formulation comprises providing a solution comprising a first solvent, a second solvent, an active agent, and an excipient. The second solvent is less polar than the first solvent and the excipient is more soluble in water than the active agent. The first and second solvents are removed from the solution to produce particles comprising the active agent and the excipient. In one version, the excipient comprises an amino acid and/or a phospholipid. A pharmaceutical formulation made by a version of the invention comprises particles comprising an active agent and an excipient which at least partially encapsulates the active agent, wherein the excipient is more soluble in water than the active agent.
US20090215783 Composition for induction or inhibition of stem cell differentiation The present invention relates to composition and methods for inducing or inhibiting differentiation of stem cells. The invention also relates to applications in the treatment of medical conditions, e.g., osteoporosis, bone fracture, bone injuries, myocardiac infarction, cardiomyopathy, degenerative muscle diseases, myopathy, and urinary incontinence.
US8754090 Use of inhibitors of bruton's tyrosine kinase (Btk) Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
WO2006121919A8 Methods of treating obsessive compulsive disorder Subjects with obsessive compulsive disorder is treated. In one embodiment, the subject is administered a compound that down regulates Group I mGluR signaling. In another embodiment, the subject is administered a compound that down regulates endocannabinoid signaling. The subject that ha obsessive compulsive disorder can further have at least one condition selected from the group consisting of fragile X syndrome, autism and mental retardation.
CN103393900A External medicament for treating lumbocrural pain and preparation method thereof The invention discloses an external medicament for treating lumbocrural pain and a preparation method thereof. The external medicament is mainly prepared from angelica, dried rehmannia root, cortex lycii radicis, cortex erythrinae, rhizoma drynariae, rhizoma cibotii, pawpaw and cyathula officinalis according to a certain weight ratio. The external medicament has the effects of expelling wind-damp, clearing and activating the channels and collaterals, nourishing the liver and kidney, curing cold, eliminating stasis to activate blood circulation and expelling toxin, and is quick in response, good in curative effect and high in cure rate when used for treating lumbocrural pain.
WO2007022934A3 Azabicyclo (3, 1, 0) hexan derivatives useful as modulators of dopamine d3 receptors The present invention relates to novel compounds of formula (I) or a salt thereof: Formula (I), wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is -CH2-, -O- or -S-; Z may be -CH- or N; A is a group P or P1, wherein P is Formula (Ia) and P1 is Formula (Ib); and Y is hydrogen, -OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substace related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
WO2008080009A2 Neuroprotection by blood flow stabilization A treatment is disclosed for alleviation or prevention of abnormal blood flow to various organs such as the eye, brain, kidneys, heart, feet and other tissues of organs with fine vascular networks that can lead to neurodegeneration as is seen in wet age- related macular degeneration (AMD), epilepsy and diabetes, in which an effective amount of a blood flow regulatory drug is administered to a subject in need of it. Illustrative blood flow regulatory drugs include anticoagulants and vasodilators, and their mixtures.
US20120184512 Gyrase and topoisomerase iv inhibitors The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.
US20120094982 1,4-benzodiazepinone compounds and their use in treating cancer The invention provides a family of 1,4-benzodiazepinone compounds and methods for their use as therapeutic agents in treating cancer. Pharmaceutical compositions and methods of making the 1,4-benzodiazepinone compounds are provided.
US20080096916 Drugs And Prodrugs Useful The Treatment Of Energy Balance In Ruminants The use of a compound of formula (I) an isomer thereof, a prodrug of said compound or isomer, or a pharmaceutically acceptable salt of said compound, isomer or prodrug, in the manufacture of a medicament for the palliative, prophylactic or curative treatment of negative energy balance in ruminants. The use of a compound of formula 1, in the manufacture of a medicament for the palliative, prophylactic or curative treatment of ruminant disease associated with negative energy balance in ruminants, wherein, preferably, the ruminant disease associated with negative energy balance in ruminants is selected from fatty liver syndrome, dystocia, immune dysfunction, impaired immune function, toxification, primary ketosis, secondary ketosis, downer cow syndrome, indigestion, inappetence, retained placenta, displaced abomasum, mastitis, (endo-)-metritis, infertility, low fertility, and lameness.
CA2680483A1 Antimicrobial solutions containing dichlorine monoxide and methods of making and using the same Methods and products are provided for treating a wound or infection in a mammal or disinfecting a surface with a hypochlorous acid solution that has been activated by a catalyst. Additionally provided is a process for preparing an antimicrobial product that produces an activated hypochlorous acid solution for use as an antimicrobial.
US20090148439 by use of a polypeptide (CD27L); in particular kidney cancer; monitoring the effectiveness of epithelial-derived cancer therapy The present invention relates to the use of a polypeptide (CD27L) for diagnosis of epithelial-related cancers, in particular kidney cancer e.g. renal cell cancer and colorectal cancer, e.g. colon cancers, as well as in methods of treatment of such cancers.
CA2701161C Lipid compositions for the treatment of gastro-intestinal disorders and the promotion of intestinal development and maturation The present invention provides a use of a lipid composition for the preparation of a nutritional, pharmaceutical or nutraceutical composition or a functional food, for the prevention and treatment of gastrointestinal diseases and disorders, and for promoting intestinal development, maturation, adaptation and differentiation.
EP1637592A1 Neuronal progenitor cells, methods to produce them and uses thereof for the therapy of neural defects A process for producing neuronal or glial progenitor cells, comprising: (a) culturing embryonic stem cells to form embryoid bodies; (b) culturing the embryoid bodies to form neural progenitor cells; (c) proliferating the neural progenitor cells in a serum-free medium containing growth factor(s); (d) further proliferating the neural progenitor cells in a serum-free medium containing growth factor(s) and isolating the neural progenitor cells; and (e) further proliferating the neural progenitor cells in a serum-free medium containing growth factor(s) and isolating the neural progenitor cells. Independent claims are included for the following: (1) a process for producing glial progenitor cells, comprising: (a) culturing embryonic stem cells to form embryoid bodies; (b) culturing the embryoid bodies to form neural progenitor cells; (c) proliferating the neural progenitor cells in a serum-free medium containing growth factor(s); (d) further proliferating the neural progenitor cells in a serum-free medium containing growth factor(s) form spheroids with neuronal and glial differentiation potential; and (e) proliferating the spheroids in a serum-free medium containing growth factor(s) until a lawn of glial progenitor cells is formed, and isolating the cells; (2) neuronal or glial progenitor cells that are produced as above and include no more than 15% of primitive embryonic cells and non-neural cells; and (3) a cell library comprising autologous and nonautologous cells as above.
WO2011015892A3 Novel crystal form of cdb - 4124 and proces s for the preparation thereof The present invention relates to novel crystalline Form II of 17α-acetoxy-21-methoxy-11β-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124), processes for the preparation thereof and pharmaceutical composition comprising it. Form II can be crystallized from different medium such as esters of C1-C4 alcohols and carboxylic acids, ketones, cyclohexane, acetonitrile, dimethylformamide, dimethyl sulfoxide, water and any mixture thereof.
CN101028365B Medicine for treating burn and ambustion and its production A medicine for treating burn and scald is prepared proportionally from the mixed liquid prepared from coptis root, scutellaria root and phellodendron bark, solution of calcium hydroxide and rapeseed oil. Its preparing process is also disclosed.
US7262172 Bactericides; therapy for infections The invention relates to novel semi-synthetic macrolides of formula (I) having antibacterial activity. More particularly this invention relates to derivatives of 8a-aza-8a-homoerythromycin A, to processes for their preparation, to compositions containing them and to their use in medicine
CN103690995A Bioabsorbable fiber, as well as preparation method and application thereof The invention relates to the technical field of functional materials, and in particular relates to a bioabsorbable fiber. The fiber comprises cellulase and bacterial cellulose, wherein the cellulose is uniformly embedded in the bacterial cellulose material. The invention also provides a preparation method of the bioabsorbable fiber. The bioabsorbable fiber is combined through twice lyophilization by utilizing the enzyme engineering, the cellulase is embedded into the bacterial cellulose, the bacterial cellulose is degraded by utilizing the cellulose, so that in vivo degradation and absorption of cellulose can be realized, the fiber is mildly degraded, the cellulose can be completely degraded, and the product glucose can be completely absorbed; the preparation method of the bioabsorbable fiber is simple, cannot destroy cellulase, does not need chemicals, does not require high-voltage and other conditions, is safe, and cannot pollute the environment.
US20120101160 Use of chemical chaperones to treat glaucoma caused by misfolded or misprocessed proteins The present invention provides methods for treating glaucoma by administering compounds capable of stabilizing misprocessed or misfolded proteins that are responsible for the condition.
USRE41065 Such as (6,7-dimethoxyquinazolin-4-yl)-(3-ethynylphenyl)-amine for treatment of hyperproliferative diseases The invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, n and m are as defined herein. The compounds of formula I are useful in the treatment of hyperproliferative diseases, such as cancer. The invention further relates to processes of making the compounds of formula I and to methods of using such compounds in the treatment of hyperproliferative diseases.
US6964968 Respiratory system disorders; cardiovascular disorders; viricides Viral infections selected from the group consisting of herpes simplex virus, varicella zoster virus, respiratory syncytial virus and cytomegalovirus can be treated by administering to the host a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof; wherein Y, Ra, and R1 are as defined herein. The compounds and salts can also be used to inhibit viral replication of these viruses in cells.
US7319134 Polypeptide having a modified amino acid sequence of a fragment of nuclear factor-interleukin 6/lymphokine activating protein; activateS various target genes, such as cytokine genes; regulation of gene expression; antiproliferative agents An alteration in phosphorylation of serine 105, within the activation domain of NF-IL6/LAP, alters its transcriptional efficacy. Polypeptides, polynucleotides and methods of use for modified transcriptional activators allow regulation of gene expression.
WO2005092393A1 Micro rna inhibiting the expression of wt1 gene and utilization of the same It is found out that a miRNA targeting the vicinity of the stop codon of WT1 gene not only inhibits the expression of the WT1 gene but also shows a remarkable effect of inhibiting the cell proliferation of a cancer cell line.
WO2013166966A1 Polymorphs of flourine-containing deuterium-substituted omega-diphenylurea or salts thereof Provided are polymorphs of flourine-containing deuterium-substituted omega-diphenylurea or of salts thereof; more specifically, polymorphs of 4-(4-(3-(4-chlorine-3-(trimethyl)phenyl)acylurea)-3-fluorine-phenoxyl)-2-(N-1',1',1'-trideuteromethyl)picolinamide, comprising a polymorph I thereof, a polymorph II thereof, and a polymorph III of a p-toluenesulfonate thereof. Said polymorphs are suitable for use in the preparation of pharmaceutical compositions that inhibit phosphokinase (such as raf kinase).
WO2013031694A1 Amine compound and salt thereof A compound represented by general formula or a salt thereof is useful as an antifungal agent. (In the formula, R1 and R2 may be the same or different and each represents a halogen atom, a cyano group, a nitro group, an optionally substituted C1-6 alkyl group or the like; R3 represents an optionally substituted pyridyl group, an optionally substituted monocyclic oxygen-containing heterocyclic group or the like; R4 and R5 may be the same or different and each represents a hydrogen atom, an optionally substituted C1-6 alkyl group or the like; X1 represents an optionally substituted 1,2-ethylene group, an optionally substituted 1,3-propylene group or the like; X2 represents an oxygen atom, a sulfur atom, a methylene group or the like; and Z1 and Z2 may be the same or different and each represents a nitrogen atom or a group that is represented by formula CH.)
WO2012063207A1 Lactam derivatives useful as orexin receptor antagonists The present invention relates to lactam derivatives of formula (I) wherein Y, R1, R2 and R3 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
CN1891287A Nano compound musk injection preparion, and its preparing method The present invention relates to a nano compound musk injection preparation and its preparation method. The pharmacological tests show that the invented nano compound musk injection preparation can be better passed through blood-brain barrier, and has delayed-release action, so that it therapeutic effect can be obviously raised.
US20050163781 uses of inhibitors against hypoxia-induced genes for the manufacture of a medicament to prevent and/or to suppress post-operative/post-wounding adhesions formation; peritoneal or pelvic cavities resulting from wound, surgery, infection, inflammation or trauma The present invention is concerned with compositions for use in the medical art. More particularly the invention relates to uses of inhibitors against hypoxia-induced genes for the manufacture of a medicament to prevent and/or to suppress post-operative/post-wounding adhesions formation. Post-operative adhesions are an unwanted result from surgery and are a major source of postoperative morbidity and mortality. The invention applies to human and veterinary applications. To date, no single therapeutic approach has proven universally effective in preventing formation of post-operative adhesions formations.
WO2007026009A1 Novel tyrosinase-specific antigenic oligonucleotides as depigmenting agents The invention concerns an antigenic oilgonucleotide hybridizing specifically with the gene encoding human tyrosinase through Hoogsteen pairing between complementary bases, said oligonucleotide forming a triple-helix structure with the human tyrosinase gene. The invention also concerns the use of said oligonucleotide as depigmenting or skin-whitening agent in a cosmetic composition or in a dermatological composition.
WO2009144483A1 Use of zolpidem for cognitive enhancement There are provided new therapeutic uses of imidazo[1,2-α]pyridine-3-acetamide derivatives, particularly relating to the modulation of theta waves in human patients..
WO2014088434A1 Application of maltotriose-coated 4th generation polypropyleneimine dendrimer ppi-g4-ds-mal-iii The application of maltotriose-coated 4th generation polypropyleneimine dendrimer PPI-G4-DS-Mal-lll containing 80-95% of peripherial amines groups coated with maltotriose particles to make a drug for treating neoplastic proliferation diseases, particularly chronic lymphocytic leukemia
US20090017011 Modulation of vegf-c/vegfr-3 interactions in the treatment of rheumatoid arthritis The present invention relates to methods for treating an individual exhibiting symptoms of chronic arthridites, as identified by an elevated level of VEGF-C expression at synovial sites, and provides materials and methods for the modulation of VEGF-C/VEGFR-3 ligand-receptor interactions as a treatment for chronic arthridites.
US20080039525 Lipid System and Methods of Use The present invention relates to a lipid system, and methods for using such a lipid system, containing specific relative ratios of omega-3, omega-6, and omega-9 fatty acids. The lipid system may be used independently or as a component of a nutritional product. A lipid system according to the present invention may contain omega-3 fatty acids, omega-6 fatty acids, and omega-9 fatty acids with the ratio of omegas-6 fatty acids to omega-3 fatty acids preferably being between 0.25:1 and 3:1, and the ratio of omega-9 fatty acids to omega-3 fatty acids preferably being between 0.4:1 and 3:1. The present invention also relates to methods for administering a lipid system or a nutritional product containing the lipid system to an individual.
US20120196818 Method for preparing polyphenol extracts from spinach leaves A method for preparing a concentrated spinach extract in a liquid or dry form and having a polyphenol titer greater than or equal to 50% is described. The method includes a step of purifying a raw spinach extract in a liquid form using a liquid-liquid extraction technique with a food oil.
WO2011111675A1 Novel indole derivative Disclosed is a compound represented by formula (1) or a pharmaceutically acceptable salt thereof useful as a therapeutic agent for diabetes and a therapeutic agent for cancer. [In the formula, R1 may either not be present or present singly or in an independent plurality and represents a halogen atom, an optionally substituted C1-8 alkyl group, a C1-8 alkoxy group, an optionally substituted amino group, hydroxyl group, cyano, nitro, carboxyl, optionally substituted acyl group, nonaromatic heterocycle group or optionally substituted carbamoyl group; R2 represents a hydrogen atom, optionally substituted C1-8 alkyl group, optionally substituted aryl group, or optionally substituted heteroaryl group.]
US7390811 Respiratory syncytial virus replication inhibitors This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH═CH—CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8). G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.
WO2006133497A1 Combination treatment The present invention relates to a method of inhibiting a virus infection in a subject. The method includes the step of administering to the subject an antiviral agent, a nucleic acid vaccine expressing an antigen of the virus, and a second vaccine including an antigen of the virus.
WO2006082456A1 Cyclohexylamides as dopamine d3 , d2 and 5ht1a antagonists The present invention relates to new dopamine D3 and D2 and serotonin 5-HT1A receptor subtype preferring ligands of formula (I); wherein A represents alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or a group of formula -NR1R2, wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, alkenyl, aryl, heteroaryl or cycloalkyl or R1 and R2 form with the adjacent nitrogen atom and optionally with further heteroatom(s) a heterocyclic ring; m is an integer of 0 to 1 ; n is an integer of 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmacological compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine and/or 5-HT1A receptors.
CN102106818B Isoliquiritigenin micro-emulsion composition The invention discloses micro-emulsion composition containing isoliquiritigenin which comprises isoliquiritigenin, emulsifying agent, assistant for emulsifying agent, oil and water. By using the composition, the solubility of the isoliquiritigenin can be greatly improved.
CN102895704A Biological activity factor composition for promoting ossification and vascularization The invention discloses a biological activity factor composition for promoting ossification and vascularization, which comprises a biological active factor and carboxylated polysaccharide, the biological activity factor is one or more selected from a bone morphogenetic protein, a transforming growth factor, a blood vessel endothelial growth factor, a basic fibroblast growth factor and an ossification protein; and the carboxylated polysaccharide is one or more selected from sulfonated chitosan, sulfonated glucan, heparin, heparin sulfate and sulfate cellulose. The invention also discloses a preparation method of a composition and a transplant containing the composition. The composition provided by the invention can promote the ossification and the blood vessel generation, can be composited with a medically acceptable carrier, and can be used in the field of bone defect repair by employing an implantation mode or an injection mode.
CN101564478A Medicament for treating peripheral facial paralysis and preparing method thereof A medicament for treating peripheral facial paralysis is made of asarum herb, prepared sichuan aconite root, scorpion, prepared arisaema root and multibanded krait. The medicament has the functions of expelling wind and cold, calming endopathic wind and vein relaxing and has marked effect in treating exposure to wind, facial paralysis and facial hemiparalysis due to main and collateral channel blockade in face. The medicament needs not to be taken orally, but treats for 10 days as one course by the gargling method. The 180 cases of clinical treatment for peripheral facial paralysis have fast acting, high effectivity up to 98.8% without any sequela. Compared with the research, the gargling therapy of the medicament is superior to the acupunctural treatment. The medicament is an externally used preparation with high safety and used for treating the peripheral facial paralysis in modern medicine.
CN103655524A Nose powder inhalation for treating epilepsy and preparation method thereof The invention discloses nose powder inhalation for treating epilepsy and a preparation method thereof. The nose powder inhalation consists of alpha-asarone powder conforming to the nasal delivery; the particle size of the powder is greater than 5 microns, but not greater than 200 microns, preferably in the range of 10-100 microns; the preparation method comprises the following steps: alpha-asarone raw materials are smashed by air streams to form the alpha-asarone powder conforming to the nasal delivery. The preparation method prepares the alpha-asarone into the powder which conforms to the requirements of the nose powder inhalation; compared with the oral preparations, the nose powder inhalation obviously improves the bioavailability while treating the epilepsy; compared with the injections, the nose powder inhalation reduces the caused allergic reactions and the patient pain caused by the injection administration as containing no accessory, decreases the distribution in the live tissue, reduces the toxic and side effects to the liver, and decreases the dosage of administration.
CN1875980A Drop pills of vepeside and preparation process thereof The invention relates to an Etoposide drop pill preparation and its preparing process, wherein the preparation is prepared from Etoposide and auxiliary constituents including medicinal adjuvant through the steps of charging Etoposide into medicinal adjuvant, homogenizing, then condensing and drying.
EP1443948B1 Process for the preparation of anthocyanin-containing products The invention provides a process for the production of an anthocyanin-containing product, said process comprising: loading an aqueous anthocyanin solution onto a cation exchange resin; flushing the resin with water; applying an acidic alkanol eluant to said resin until anthocyanin begins to elute therefrom whereafter applying a non-acidic alkanol eluant to said resin; collecting anthocyanin-containing eluate from said resin; evaporating off alkanol from said eluate adding water and if necessary an anticoagulant to the eluate to produce an aqueous anthocyanin solution, preferably a solution containing at least two anthocyanins; spray-drying said solution; and optionally coating the spray dried product.
US7456163 Macrocycles useful in the treatment of alzheimer's disease The present invention is macrocycles of the formula (X): for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme for the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
WO2006127595A1 5-aminopyrazole carboxylic acid derivatives and methods of treatment of metabolic-related disorders thereof The present invention relates to certain pyrazole carboxylic acid or ester derivatives of Formula (I) and pharmaceutically acceptable salts thereof which exhibit useful pharmacological properties, for example, as agonists for the GPCR referred to herein as RUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, such as, dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
US20080139667 Pharmaceutical Compositions For the Treatment of Disease and/or Symptoms in Arthritis The invention relates to the use of a combination of cannabinoids for the treatment of pain, inflammation and/or disease modification in arthritis. Preferably the cannabinoids are selected from cannabidiol (CBD) or cannabidivarin (CBDV) and delta-9-tetrahydrocannabinol (THC) or tetrahydrocannabinovarin (THCV). More preferably the cannabinoids are in a predefined ratio by weight of less than or equal to 19:1 of CBD or CBDV to THC or THCV.
CN102008427A Latanoprost ophthalmic in situ slow release gel The invention provides a novel Latanoprost ophthalmic in situ slow release gel which is used for local treatment of open angle glaucoma and the patients with too high intraocular pressure which are difficult to treat or endure by other medicaments. The medicament can solve the problems of short detention time in the eye and low bioavailability of the ordinary eye drop, and overcomes the problems that the ordinary ophthalmic gel is lack of good spreadability and the dose is difficult to control. The bioavailability of the ophthalmic medicine is improved from 1%-3% to 15%-20%. The preparation exists in vitro in a liquor form, and is converted into gel when dropping in the eyes. The Latanoprost ophthalmic in situ slow release gel has slow release function, and provides evidence for the clinical popularization of the ophthalmic slow release preparation.
CN103263393A Ardipusilloside I slow-release implant tablets and preparation method thereof The invention discloses ardipusilloside I slow-release implant tablets serving as an anti-glioma medicament and a preparation method thereof. The ardipusilloside I slow-release implant tablets prepared by using the method are prepared from the following components in percentage by weight: 0.6 to 3.5 percent of ardipusilloside I, and 96.5 to 99.4 percent of biodegradable medicament-carrying polymer, wherein the weight percentage sum of the components is 100 percent. The implant tablets are prepared by adopting the preparation method comprising the steps of preparing microspheres from the ardipusilloside I and the medicament-carrying polymer and then tabletting, and are tablets capable of being implanted into the craniocerebral focus part. Through the degradation of the polymer in vivo, the ardipusilloside I can be slowly released to the craniocerebral tumor part at certain rate away from the blood brain barrier, the toxic reaction of the whole body is reduced, the bioavailability is improved, and the implant tablets have good biocompatibility.
CN101991768A Compound medicament for treating and preventing halitosis The invention relates to a compound medicament for treating and preventing halitosis, which is especially suitable for treating halitosis with high repeatability after healing. The invention provides the compound medicament for treating and preventing halitosis, which effectively prevents halitosis, has low repeatability without side effect on human and is prepared from the following raw materials in parts by weight: 0.5-2 parts of asarum, 2-3 parts of cimicifuga foetida, 2-4 parts of wild ginger, 3-5 parts of agastache rugosa leaves, 1-3 parts of nard, 2-3 parts of angelica root, 1-2 parts of calcitum, 3-6 parts of plaster, 2-4 parts of the root of kudzu vine, 2-4 parts of root of common peony, 5-8 parts of hairyvein agrimonia herb and bud, 3-6 parts of sugar stevia leaves, 2-4 parts of mint, 2-6 parts of common salt, 5-8 parts of blackberrykiky rhizome, 1-4 parts of dark plum fruit, 5-8 parts of ballonflower, 2-5 parts of ophiopogon root, 3-8 parts of liquorice root, 0.5-1.5 part of pseudo-ginseng, 1-3 parts of osmanthus and 2-5 parts of calcite.
US6933373 Tumor suppressor protein for as a antiproliferative agent Proteins derived from the product of tumor suppressor gene p53 and having enhanced functions for therapeutical use are disclosed. The proteins advantageously have enhanced tumour suppressor and programmed cell death inducer functions, particularly in proliferative disease contexts where wild-type p53 protein is inactivated. Nucleic acids coding for such molecules, vectors containing same, and therapeutical use thereof, particularly in gene therapy, are also disclosed.
CN103110702A Navel-warming paste capable of warming spleen and stomach for dispelling cold and preparation method thereof The invention belongs to the technical field of a medicine, and in particular relates to a navel-warming paste capable of warming the spleen and the stomach for dispelling cold and a preparation method thereof. The navel-warming paste capable of warming the spleen and the stomach for dispelling cold is characterized by being mainly prepared from the following crude medicines: 20-25 parts of cinnamon, 10-15 parts of white pepper, 20-25 parts of pericarpium granati, 20-25 parts of fructus chebulae, 20-25 parts of Chinese gallnut, 5-7 parts of clove, 0.5-0.75 parts of a raceanisodamine hydrochloride tablet and 235-250 parts of yellow lead. The navel-warming paste disclosed by the invention has the beneficial effects of combining various medicines to warm the spleen and the stomach for dispelling cold as well as to relieve diarrhea and paint; the navel-warming paste has remarkable effect on treating acute and chronic abdominal pain and diarrhea, dyspepsia, inappetence and night sweat caused by pathogenic cold, and the cure rate is 90%; the navel-warming paste can cure generally by 1-2 courses of treatment, so that the course of disease is effectively shortened and paint of the patient is rapidly removed.
CN101416977A Preparation method of azalide type tulathromvcin injection The invention relates to a preparation method of an injection containing azalide tulathromycin; the injection consists of tulathromycin, hydrochloric acid, propylene glycol, phenol and water used for injection. The preparation method comprises the steps of: adding a proper amount of the water used for injection into a stainless-steel liquid distributing tank, adding 5100g of a 10-percent (w/w) hydrochloric-acid water solution and stirring the solution evenly, slowly adding 104g to 208g of the tulathromycin into the solution, stirring the solution till the tulathromycin is dissolved, adding the 10-percent (w/w) hydrochloric-acid water solution to adjust the pH value to be 4.0 to 7.0, heating the solution to the temperature of 60 DEG C to 70 DEG C for 10min to 30min, adding and evenly stirring 500g of propylene glycol (a cosolvent) when the temperature reaches 25 DEG C, adding the 10-percent (w/w) hydrochloric-acid water solution to regulate the pH value to reach 5.4, adding 5g to 10g of the phenol as a preservative, adding the water used for injection till the total volume of the solution is adjusted to be 1000ml, filtering the solution by a 5-to-10-micron filter and a 0.45-micron filter in sequence, encapsulating the filtered preparation and sterilizing the preparation by a wet-heat high-pressure sterilizing method for 30min at the temperature of 121 DEG C.
WO2009152920A1 3-(3-pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazine derivatives as met kinase inhibitors Compounds of the formula (I) in which R1, R2, R3, R3', R4 are each as defined in claim 1 are inhibitors of tyrosine kinases, especially of Met kinase, and can be used for treatment of tumours among other uses.
US20070281005 Administering zonisamide; clearing mucus; protective patches A method of treating or preventing Obstructive Sleep Apnea (OSA) comprises the administration of a pharmacologically effective amount of zonisamide to a patient in need thereof, with the proviso that OSA caused by external mechanical obstruction of the airways, such as by mucus, is excluded. Also disclosed is the use of zonisamide for the manufacture of a medicament useful in the treatment; a protective patch comprising zonisamide and a pharmaceutically acceptable carrier for transdermal or transmucosal administration to a person suffering from OSA; and the use of zonisamide for the manufacture of a diagnostic device, kit or composition for the diagnosis of sleep disordered breathing.
CA2543342A1 Combination treatment of obesity involving 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity and lipase inhibitors The present invention relates to a novel medical use of 4,5-dihydro-1 H~ pyrazole compounds which are potent antagonists of the cannabis CB1-receptor in combination with lipase inhibitors. Said compounds are particularly suitable in combination with lipase inhibitors in the manufacture of medicaments for the treatment and/or prophylaxis of obesity in adolescent or in juvenile patients and/or for the treatment and/or prophylaxis of drug induced obesity in juvenile as well as in adolescent patients. The compounds have the general formula (I) wherein the group Bb represents sulfonyl or carbonyl, and the substituents R, R1, R2and R3, and the group Aa are defined as shown in the description. Preferred lipase inhibitors are orlistat, panclicins, ATL-962 and/or lipstatin.
US20110118339 Chemically modified oligonucleotides and uses thereof This invention relates generally to chemically modified oligonuceotides useful for augmenting activity of microRNAs and pre-microRNAs. E.g., the invention relates to single stranded chemically modified oligonuceotides for augmenting microRNA and pre-microRNA expression and to methods of making and using the modified oligonucleotides.
US20090215009 Medical material, artificial tooth root, and method of producing medical material [Problems] To provide a medical material having such a structure that enables even diffusion and distribution in the material of a sufficient amount a substance necessary for a medical treatment. [Means for Solving Problems] A medical material 10 composed of a porous three-dimensional construct 11, which is a rectangular parallelepiped having a porosity of from 20 to 97% and pores 12, 13, 14 and 15 provided in the main body. From this pore 12, a substance such as calcium phosphate or ceramics apatite and/or a physiologically active cell, tissue or protein and a substance suitable for exerting the functions thereof are introduced.
CN101721402A treating bone-related disorders with selective androgen receptor modulators This invention provides a method of treating, preventing, suppressing, inhibiting, or reducing the risk of developing a bone-related disorder, for example osteoporosis, osteopenia, increased bone resorption, bone fracture, bone frailty and/or loss of bone mineral density (BMD), by administrating a therapeutically effective amount of a selective androgen receptor modulator (SARM) and/or its analogue, derivative, isomer, metabolite pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof. The invention also provides methods of decreasing fat mass (FM) and increasing lean mass, comprising administering same.
US20120258046 Mannose-containing solution for lyophilization, transfection and/or injection of nucleic acids The present invention is directed to (the use of) a solution containing at least one nucleic acid (sequence) and free mannose for lyophilization, transfection and/or injection, particularly of RNA and mRNA. The inventive solution exhibits a positive effect on stabilization of the nucleic acid (sequence) during lyophilization and storage but also leads to a considerable increase of the transfection efficiency of a nucleic acid. It thus also increases in vivo expression of a protein encoded by such a nucleic acid upon increased transfection rate. The present invention is furthermore directed to a method of lyophilization using the mannose-containing solution, to pharmaceutical compositions, vaccines, kits, first and second medical uses applying such a mannose-containing solution and/or a nucleic acid (sequence) lyophilized or resuspended with such a solution.
WO2006118299A1 Gpcr inhibitor One or more members selected from cysteine, methionine, ornithine and derivatives containing a skeleton of any of these amino acids are used as an inhibitor of GPCR such as a serotonin receptor, a histamine receptor or a muscarinic receptor.
US7608633 1-(4-Octylphenoxy)-3-(pyrrol-1-yl)propan-2-one, for example; for preventing and treating diseases caused by an increased activity of this enzyme, such as inflammation, pain, fever, allergies, asthma, psoriasis and endotoxic shock The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds.
WO2010057848A1 8-azabicyclo [3.2.1]oct-2-ene derivatives and their use as mono-amine neurotransmitter re-uptake inhibitors The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
CN102755338A Compound preparation containing fosaprepitant and palonosetron hydrochloride, and preparation method thereof The invention provides a sterile lyophilized compound preparation containing fosaprepitant and palonosetron hydrochloride, and a preparation method thereof. According to the invention, effective dosages of fosaprepitant dimeglumine and palonosetron hydrochloride are adopted as effective components, and auxiliary materials such as a solubilizer, a complexing agent, an excipient, and an acidity adjusting agent are contained in the preparation. The preparation is filtered, sterilized, sub-packaged, and lyophilized. When in use, the sterile lyophilized compound preparation provided by the invention is added into a solvent, such that injection solution with an appropriate concentration is prepared and can be used. With one time of medication, clinical demands of two treatment medicines can be satisfied, such that patient compliance is improved. The preparation method of the compound preparation is simple, and the method is suitable for industrialized productions.
WO2005082374A1 Predictors for patients at risk for glaucoma from steroid therapy The present invention provides a method to evaluate a patient's risk for increased intraocular pressure after receiving intraocular steroid therapy comprising the steps of: (a) administering to an eye a steroid at a challenge dose ranging from about 50 µg to about 800 µg; and (b) determining the intraocular pressure changes thereafter.
US7250403 Administration of immunomodulatory polynucleotide microcarrier complexes featuring a polynucleotide comprising at least one immunostimulatory sequence bound to a biodegradable microcarrier or noncarrier The invention provides new compositions and methods for immunomodulation of individuals. Immunomodulation is accomplished by administration of immunomodulatory polynucleotide/microcarrier (IMP/MC) complexes. The IMP/MC complexes may be covalently or non-covalently bound, and feature a polynucleotide comprising at least one immunostimulatory sequence bound to a biodegradable microcarrier or noncarrier.
US7528164 e.g. 2-Amino-4-(3-bromo-4,5-dimethoxyphenyl)-3-cyano-7-methyl-4H-pyrrolo [2,3-h]chromene; antiproliferative, antitumor, anticarcinogenic agent The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the Formula (I): wherein R1, R3-R5, A, D, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
CA2377373C Nitric oxide donors for inducing neurogenesis There is provided a method of promoting neurogenesis by administering a therapeutic amount of a nitric oxide donor compound to a patient in need of neurogenesis promotion. Also provided is a compound for providing neurogenesis having an effective amount of a nitric oxide donor sufficient to promote neurogenesis. A nitric oxide compound for promoting neurogenesis is also provided. Further, a method of augmenting the production of brain cells and facilitating cellular structural and receptor changes by administering an effective amount of a nitric oxide donor compound to a site in need of augmentation is provided. There is provided a method of increasing both neurological and cognitive function by administering an effective amount of a nitric oxide donor compound to a patient.
WO2012031563A1 Heterocyclic amino berbamine derivatives, preparation method and use thereof Heterocyclic amino berbamine derivatives having formula (I) or their pharmaceutically acceptable salts, processes for preparing them, pharmaceutical compositions comprising them, and their use in manufacture of antitumor medicaments are provided.
US7491716 Glycogen synthase kinase-3 inhibitors such as [1-(4-Imidazo[1,2-a]pyridin-3-yl-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl)-6,7-dihydro-6H-[1,4]diazepino[6,7,1-hi]indol-6-yl]-[morpholin-4-yl]methylenecyanamide, used for treating diabetes, Alzheimer's disease and for stimulating bone deposition in mammals The present invention provides kinase inhibitors of Formula I.
EP2533786A2 Methods and compositions to improve mechanical resistance of teeth Provided are compositions and methods for preventing dental caries, as well as aqueous compositions and methods for improving the mechanical strength of teeth.
EP0861266B3 Peptide conjugates derived from thymic hormones, their use as medicament and compositions containing them The invention relates to peptide conjugates comprising a sequence of at least 3 amino acids derived from a thymic hormone selected amongst thymuline and thymopoïetine, the amino acids being independently in the form D, L or DL, said sequence being chemically or physically conjugated with at least one compound selected amongst monocarboxylic acids having the general formula (I): HOOC-R, as well as alcohol, aldehyde or amide derivatives, the dicarboxylic acids having the general formula (II): HOOC-R1-COOH. The invention also relates to the use of such conjugates as medicaments, and pharmaceutical or cosmetological compositions containing them.
CN101628086B Gastrodiaelata Blume plant extract for preventing and treating vascular dementia and preparation method thereof The invention relates to application of a Gastrodiaelata Blume plant extract containing parishin derivants on preparing a medicament for preventing and treating vascular dementia and other diseases. The invention also relates to a method for preparing the plant extract extracted and refined from Gastrodiaelata Blume plant, wherein active components are the parishin derivants, in particular to parishin A, B and C. The method adopts alcohol extraction; and an extract is refined and purified by a chromatogram method to obtain the plant extract with the content of the parishin derivants of 35 percent, in particular over 50 percent. A medicament preparation optimally selects injections, troches, capsules, soft capsules, oral liquid or dropping pills and the like.
CN101172142B Medicament for treating carbuncle, gangrene, turgescence toxin and skin ulcer, and method of producing the same The invention relates to a medicine for curing carbuncle, cellulitis, pyogenic infection and skin ulcer, which is formed by manufacturing szechuan aconite, kusnezoff monkshood, forsythia, dried rehmannia root, frankincense, common myrrh tree, semen momordicae, cassia bark, dragon blood, mercury powder, red lead and sesame oil. When the medicine is manufactured, weighed medicinal materials are immerged into the weighed sesame oil for two hours to five days, and the medicinal materials are heated to fry to be brown, then the fried medicinal materials are filtered, and are ceaselessly stirred after being added with the red lead, a finished product is obtained after being cooled. Because the medicine components used for manufacture the medicine of the invention is fewer, and the price of eachcomponent is cheaper, the cost of the medicine is lower; the medicinal materials generates good treatment effect after being composed rightly; the medicine of the invention has the advantage that themanufacture process is simpler.
US20110237575 Inhibitors of fatty acid binding protein (fabp) The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below: (I)
US20120183527 Measurement of anti-amyloid antibodies in human blood The present invention provides improved immunoaffinity methods for detecting high avidity anti-amyloid antibodies present in a biological sample. In other aspects, the present invention provides methods for diagnosing diseases associated with amyloid proteins. Also provided by the present invention are methods for identifying candidates likely to respond to treatment comprising administration of an immunoglobulin preparation.
US7709481 peroxisome proliferator activator receptor (PPARdelta) agonist; type-2 diabetes, atherosclerosis, cardiovascular disorders; 3-{2-Chloro-4-[4-methyl-2-(1-methyl-cyclohexyl)-oxazol-5-ylmethoxy]-phenyl}-4H-[1,2,4]oxadiazol-5-one The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula: wherein the substituents R1-R5 and R7-R10 are defined herein. The compounds are therapeutically effective in the regulation and modulation of lipid and carbohydrate metabolism in mammals and are thus suitable for the treatment of diseases such as type-2 diabetes, atherosclerosis, cardiovascular disorders and the like.
US7176217 such as N-Hydroxy-2-[(4-methoxyphenyl)sulfonyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide, used in cosmetics or drugs as gelatinase inhibitors, for preventing skin aging or wrinkling; preventing diseases due to abnormal metabolism of tissue matrices such as arthritis, ulcers, metastasis or tumors An azabicyclo compound (I) or a salt thereof in accordance with the present invention has an excellent inhibiting action on matrix metalloproteases (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions. wherein R is H, alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, acyl, COOR1, carbamoyl or SO2R2 (wherein R1 and R2 each are alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl); X is methylene, ethylene or propylene; and is a single bond or a double bond.
EP1282402B1 Stabilized aqueous suspensions for parenteral use A pharmaceutical aqueous suspension formulation for parenteral administration having substantially stabilized pH, comprising a biologically active compound and a pH controlling effective concentration of L-Methionine. Preferably, the biologically active compound is a steroidal compound, for instance exemestane, medroxyprogesterone acetate and estradiol cypionate or a combination of medroxyprogesterone acetate and estradiol cypionate.
US20110281892 Method and formulation for cold treatment in adults and children with increased safety Methods and dosage formulations for the safe treatment of cold, cough, flu, and sinus symptoms in children and adolescents by age and nature of symptoms, and adults and the elderly by age, nature of symptoms, and concomitant patient medical conditions. The method of the present invention comprises the formulation of a cold medication which consists essentially of combinations of a nonsedating or minimally sedating antihistamines with pain relievers and the expectorant, guaifenesin.
WO2014043110A3 Crosslinked polymer nano-assemblies and uses thereof The invention provides powerful methods and compositions for designing, selecting, fine-tuning and optimizing polymer nanogel and other supramolecular assemblies for various properties including, for example, particle size, density and morphology, guest loading capacity and encapsulation stability, and dynamic release control.
US20120329736 Treatment for gastrointestinal disorders using a selective, site-activated binding system The teachings provided herein generally relate to site-activated binding systems that selectively increase the bioactivity of phenolic compounds at target sites. More particularly, the systems taught here include a phenolic compound bound to a reactive oxygen species, wherein the phenolic compound and the reactive oxygen species react at a target area in the presence of an oxidoreductase enzyme.
EP1778361A1 Antimicrobial and/or antiviral composition and to methods for preparing and administering same The present invention provides for an antimicrobial and/or antiviral composition suitable for administration to a surface. The antimicrobial and/or antiviral composition is suitable for administration to a surface, comprising an essential oil portion; and an effective amount of a volatile liquid carrier such that a majority of the composition readily evaporates after dispersal onto the surface. The composition is compatible with and suitable for topical use with human skin. Methods of preparing and administering the antimicrobial and/or antiviral compositions are also disclosed.
CN102993158A Genipin derivative and application thereof The invention belongs to the field of preparation of new compounds and in particular provides a genipin derivative as well as a preparation method and an application thereof. The genipin derivative and pharmaceutically acceptable salt thereof are shown as a general formula I (described in the specification), wherein R1 is one selected from C1-6 alkyl or alkyl amino, C1-20 aryl, C1-20 aromatic amino and C1-6 heterocyclic amino; R2 is one selected from C1-6 alkyl, C1-20 aryl, C1-6 heterocycle and an amino group; R3 is one selected from C1-6 alkyl, C1-20 aryl, C1-6 heterocycle, methylsulfonyl, p-tosyl group and -COR4, and R4 is one selected from C1-6 alkyl, C1-20 aryl, C1-6 heterocycle and the amino group. The derivative provided by the invention has application value in preparation of medicine used for treating diabetes mellitus II.
US7060290 Phosphocholine linked prodrug derivatives Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substituted or unsubstituted alkanoyl, (iv) substituted or unsubstituted alkenoyl wherein the double bond is cis, and (v) (ortho or para) carbonyl-substituted aryl; and wherein the subtituent is each an independent group or linked together thereby forming a ring; and wherein X is one or more substituted or unsubstituted group containing one or more O, N, or S atom and wherein the substituent is each an independent group or linked together thereby forming a ring; and wherein the therapeutic agent is an alcohol-containing water-insoluble steroids or another alcohol containing compounds and methods to prepare such compounds.
US20110027215 Protein-based polymer tissue adhesives for medical use Tissue adhesives formed by crosslinking albumin and/or gelatin with certain polyamines and/or polycarboxylates using a water-soluble carbodiimide are disclosed. The use of the tissue adhesives for medical and veterinary applications such as topical wound closure; and surgical procedures, such as intestinal anastomosis, vascular anastomosis, tissue repair, and ophthalmic procedures; drug delivery; anti-adhesive applications; and as a bulking agent to treat urinary incontinence are described.
CA2602583A1 Biaryl derived amide modulators of vanilloid vr1 receptor The invention is directed to novel vanilloid receptor type 1 (VR1) ligands. More specifically, the invention relates to novel biaryl-derived amides that are potent antagonists or agonists of VR1. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
CN103099795A Indometacin sustained release tablet, preparation method thereof, as well as release controlling method and standard The invention relates to an indometacin sustained release tablet, a preparation method thereof, as well as a release controlling method and standard. The indometacin sustained release tablet is prepared from the following components in percentage by weight: 8.0-25.0% of indometacin, 25.0-40.0% of hydroxypropyl methyl cellulose, 12.0-25.0% of microcrystalline cellulose K15M-CR, 8.0-15.0% of microcrystalline cellulose, 15.0-25.0% of lactin, 1.0-6.0% of gum acacia and 0.5-1.5% of magnesium stearate. A full-powder direct compression process is adopted; the production process is simplified; the methoxyl content of prepared mid-product methoxyl is 8.2-18%; and the propoxyl content is 2.6-7.8%. The quality of the indometacin sustained release tablet disclosed by the invention reaches the standard; a reference product has release similarity; mass control is carried out before production; rework can be reduced; the production cost is saved; the energy consumption is reduced; and the production efficiency is improved.
WO2014143768A1 Tricyclic heterocycles as bet protein inhibitors The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
CN103463035A Application of Lycojaponicumin B in anti-herpes virus medicine The invention discloses an application of Lycojaponicumin B in preparation of an anti-herpes virus medicine. As shown in experiments, the Lycojaponicumin B has an excellent inhibitory effect on Herpes simplex virus HSV-1 and Herpes simplex virus HSV-2, which indicates that the Lycojaponicumin B has a potential application value in the field of treating herpes virus infection diseases, and the invention provides experimental basis for clinic use of the Lycojaponicumin B for treating the herpes virus infection diseases, provides certain guidance for research on a medicine preventing HSV-1 and HSV-2 virus and has an important reference value.
US20110220265 Preparation for External Use A preparation for external use which, even when ingredients such as a drug, absorption accelerator, and plasticizer are contained therein in a large amount, is excellent in pressure-sensitive adhesive properties including cohesive force and which, when a drug is contained therein, enables the drug to have excellent percutaneous absorbability. The preparation for external use includes a pressure-sensitive-adhesive matrix layer, wherein the pressure-sensitive-adhesive matrix layer comprises a pressure-sensitive adhesive base comprising a hydroxylated polymer, a boron compound, and silicic acid.
WO2012118492A1 Heterocyclic sulfonamides as raf inhibitors Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I), stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
CA2175215C Semisynthetic analogs of rapamycin (macrolides) being immunomodulators Novel macrolide compounds, semisynthetic analogs of Rapamycin, of formula (I) and pharma-ceutically acceptable salts, esters, amides and pro-drugs thereof, processes for the preparation of the compounds of the invention, intermediates useful in these processes, a pharmaceutical composition, and a method of treating immunomodulatory disorders are disclosed.
CN102134225A Tricyclic diterpene lactone and preparation method and application thereof The invention belongs to the field of organic chemistry, and more particularly relates to tricyclic diterpene lactone, the molecular structure of which is shown as formula (I). the compound can be prepared b the following method: (1) taking Rhizoma Atractylodis Macrocephalae decoction pieces, adding a proper amount of ethyl acetate for soaking and extraction for 1-3 times at room temperature, soaking and extraction each time lasts for ten days, an ethyl acetate extracting solution is combined, ethyl acetate is recovered by decompression to obtain an extractum; (2) dissolving the extractum in the ethyl acetate, adding silica gel GF254 with the weight 2-3.5 times of that of the extractum, mixing uniformly, thoroughly volatilizing the ethyl acetate, and obtaining a sample-injected silica gel; filling blank silica gel with the weight 1-3 times of that of the sample-injected silica gel into a chromatographic column and then filling the sample-injected silica gel; conducting continuous gradient elution to an eluent formed by petroleum ether and absolute ethyl alcohol with the flow rate of 0.3 to 10mL/min, collecting crystals separated out from fraction of absolute ethyl alcohol with the volume concentration of 0-0.5 percent in the petroleum ether, and then obtaining tricyclic diterpene lactone. The compound can be used for preparing medicaments for propelling bone mesenchymal stem cells to disperse to cartilage.
WO2007141200A8 Novel n-aryl and n-heteroaryl substituted pyridinone derivatives for use in mch-1 mediated diseases The present invention concerns N-aryl and N-heteroaryl substituted pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.
US20120108532 Pharmaceutical composition for neuroprotective treatment in patients with ictus comprising citicoline and uric acid A pharmaceutical composition comprised of uric acid and citicoline is for the neuroprotective treatment of patients with ictus.
EP0831847B1 Method of synthesis of di-beta-d-glucopyranosylamine compounds for controlling inflammatory reactions Adverse inflammatory reactions can be treated by administrating to an organism a composition having diglucosylamine as the active ingredient. The preferred compound is di-Beta-D-glucopyranosylamine. A simple method for making diglucosylamine in high purity is obtained by reacting glucose, a nitrogen containing base, and either methanol or ethanol to form the diglucosylamine and then recovering the diglucosylamine preferably with the use of charcoal. The preferred diglucosylamine, di-Beta-D-glucopyranosylamine, has extraordinary anti-inflammatory activity. It can be formulated with a pharmaceutically acceptable carrier to make pharmaceutical compositions which are effective in treating inflammations. This pharmaceutical composition can also be used to treat adverse inflammatory reactions that are the result of the disruptions of a dynamic network of cellular mechanisms in organisms. In addition, application of this composition also serves to reestablish the balance of the cellular defense network in an organism which has its cellular defense network out of balance. In this unbalanced case, the composition serves to treat the pathology of inflammation and activates the inflammatory control system in vivo. These adverse inflammatory reactions can also be treated by administrating to the organism glucose in the presence of NH3<+> ions and at a pH of about 7.0 or greater. The glucose can preferably be applied by orally administrating an enteric-coated form of glucose, alone or in combination with other medicaments.
US20120107304 Combination therapy in treatment of oncological and fibrotic diseases The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of a cell signalling and/or angiogenesis inhibitor in conjunction with an Aurora kinase inhibitor.
US7585520 Compositions containing both sedative and non-sedative antihistamines and sleep aids Compositions containing both a sedative compound and a non-sedative antihistamine are provided. More particularly, compositions for administration at bedtime containing a sedating antihistamine or other sedating compound in immediate release form and a non-sedating antihistamine in delayed-release form are described. Alternatively, a composition, for administrating upon awakening, containing a non-sedating antihistamine in immediate release form, and a sedating antihistamine or other sedative in delayed-release form is described. Methods of inhibiting the release of histamines by administration of the compositions to a mammalian subject are also provided. The dosage forms may comprise other medications, such as leukotriene receptor antagonists, to enhance the suppression of histamine symptoms.
CN103040842A Prostaglandin pharmaceutical composition and prostaglandin medicament suppository prepared by the prostaglandin pharmaceutical composition The invention discloses a prostaglandin pharmaceutical composition, containing 1 part by weight of prostaglandin medicament, and 1-300000 parts by weight of fat, wherein the fat is a mixture selected from one or more of cocoa butter, semisynthetic cocounut oil ester, semisynthetic litsea cubeba fat, mixed fatty glyceride, semisynthetic palm oil ester, propylene glycol stearate and lanolin. The technology effects of the invention reside in that: the misoprostol is catalyzed by water for degrading; the auxiliary material, of common preparation is hydrophilic, the fat is used as an auxiliary material, which greatly reduces the probability for the misoprostol to contact water, achieves unexpected effects, and significantly raises the stability in a storage period.
CN103087043A Benzamide derivative resisting proliferative activity and pharmaceutical preparation thereof The invention discloses a novel benzamide derivative represented by the formula (I), wherein various substituent groups Het, G1, G2, G3, Y, X1, X2, X3 and X4 are defined in the specification. Furthermore, the invention further discloses preparation methods of the compounds, pharmaceutical compositions containing the compounds, and the purposes of the compounds as active components of medicines for treating diseases related to proliferation, such as leukemia and solid tumours.
WO2009115272A1 Remineralizing dental care product and method for the production thereof A method for producing a remineralizing dental care product, comprising the following steps: a) completely dissolving at least one organic calcium salt, selected from the group of physiologically acceptable organic acids, in warm water at 35-80ºC; b) concentrating the solution by evaporation at reduced pressure at a hot bath temperature of 50-150ºC; c) depressurizing to normal pressure and subsequently adding at least one organic acid at constant temperature; d) concentrating the solution by evaporation at reduced pressure at a hot bath temperature of 50-150ºC; e) depressurizing the hot, flowable calcium salt hydrate melt to normal pressure; aa) charging a toothpaste basic composition, comprising: 24-45% by weight water; 25-45% by weight humectant; 0.5-3% by weight binding and thickening agent; bb) producing a mixture of the toothpaste basic composition while heating to a temperature range of 40 to 70ºC; cc) adding the calcium salt hydrate melt to a base composition the temperature of which is controlled at 40 to 70ºC, with subsequent stirring until a homogeneous dental care mixture is obtained, wherein the proportion of the calcium salt hydrate melt relative to the total weight of the dental care mixture is between 7 and 49.5% by weight, and the sum of the volume information of the constitutes starting with step aa) adds up to 100%; dd) cooling off the dental care mixture.
CA2231292C Method for decreasing ldl-cholesterol concentration and increasing hdl-cholesterol concentration in the blood to reduce the risk of atherosclerosis and vascular disease A method of altering the concentration of cholesterol constituents in human blood is provided. A daidzein material is administered to a human to increase the concentration of HDL-cholesterol and to decrease the level of LDL-cholesterol in the blood. The daidzein material may be administered in a pharmaceutical composition, or in a dietary supplement, including soy protein based dietary supplements. Utilization of daidzein to increase the concentration of HDL cholesterol and to decrease the concentration of LDL-cholesterol in the blood reduces the risk of atherosclerosis and vascular disease by providing more health beneficial HDL-cholesterol and reducing the level of atherosclerosis-inducing LDL-cholesterol.
CN1768734A Sodium ferulate glucose infusion liquid and its preparation method The invention relates to ferulae acid sodium glucose liquid and its producing method. It is characterized in that it is made from ferulae acid sodium (C10H9NaO4*2H2O), glucose and stabilizing agent, while the weight proportions are: ferulae acid sodium at 90-110mg, glucose at 4500-5500mg, and the stabilizing agent at 10-100mg, to be added with asepsis injection water to 100ml. The preparing method comprises: adding the glucose as said weight proportion into asepsis injection water and injection active carbon to be boiled and mixed with heat-insulation; then adding the ferulae acid sodium and stabilizing agent as said weight proportion to be mixed and dissolved; filtering and adding asepsis injection water to full content; adjusting the pH valve to 4.0-6.0; accurately filtering, charging nitrogen, sealing, and moist heat steam sterilizing at 115Deg. C for 30 minutes to attain the ferulae acid sodium glucose liquid. The invention has significant curative effect, better stability and litter bad effect, and it has simple operation, lower cost and wider drug source.
WO2007104560A1 Substituted 4-amino-quinazoline derivatives as regulators of metabotropic glutamate receptors and their use for producing drugs The invention relates to substituted 4-amino-quinazoline derivatives of formula (I), to methods for producing them, to drugs containing said compounds and to their use for producing drugs.
CN103330692A Simvastatin component improving stability and preparation method thereof The invention relates to a simvastatin component improving stability and a preparation method thereof. The component comprises simvastatin, starch, lactose, hydroxypropylcellulose, hydroxypropyl methylcellulose, magnesium stearate and sodium carboxymethyl starch which are used to prepare simvastatin by direct tabletting. The medical simvastatin prepared by the invention is good in appearance of tablets and hardness and level and smooth in appearance, and the dissolution rate reaches over 80%. With the adoption of simple process of mixing powder and tabletting, the production cost can be lowered, and the component is suitable for industrialized production in a large scale.
CN103524524A New compound in fructus schizandrae as well as preparation and application method of new compound The invention belongs to the technical field of medicaments, and specifically relates to a new compound in fructus schizandrae as well as a preparation method and an application of the new compound. The new compound disclosed by the invention has a molecular formula of C30H38O11, and the preparation method specifically comprises the following steps of extracting stems or leaves of fructus schizandrae by using ethanol at normal temperature to obtain an extractum; suspending the extractum by using water, and then extracting the extractum by using petroleum ether and acetic ether in sequence; taking an acetic ether extract, and performing chromatographic separation on the acetic ether extract by using an SEPHDEXLH-20 column; taking a 55-65% methanol/water part solvent, and then performing chromatographic separation by using a silica gel column; combining the petroleum ether extract with the acetic ether extract according to a ratio of 80:20-50:50, then performing separation by using a semi-preparative high performance liquid chromatography, setting the detection wavelength to be 270-280nm, collecting methanol and a water part according to a ratio of 45:55-55:45, and performing crystallization to obtain the new compound, namely fructus schizandrae dilactone ketone A. The new compound disclosed by the invention is used for preparing anti-hepatoma drugs.
CN101036636A Method for increasing the oral bioavailability of S-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]-2-methylpropanethioate The invention provides pharmaceutical compositions comprising a cholesteryl ester transfer protein (CETP) inhibitor and a water-insoluble concentration-enhancing additive, which exhibit improved bioavailability. The invention also provides methods of treating cardiovascular disorders comprising the administration of the pharmaceutical compositions comprising a CETP inhibitor.
CN1846676A Slow-released injection containing fluoroplex synergist and its prepn process The slow released anticancer injection containing 5-FU consists of slow released microballoon and solvent. The slow released microballoon includes effective anticancer component and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The effective anticancer component is 5-FU synergist or the combination of 5-FU and its synergist; the 5-FU synergist is selected from phosphorinositide 3-kinase (PI3K) inhibitor, pyrimidine analogue and DNA repair enzyme inhibitor; the slow releasing supplementary material is PLA, PLGA, EVAc, etc or their composition; and the suspending agent is sodium carboxymethyl cellulose, mannitol, etc. The slow released microballoon may be also prepared into slow released implantation preparation. Implanting or injecting the slow released preparation to local tumor part can lower the systematic toxic reaction of the medicine and raise the medicine concentration of local tumor part selectively to raise the treating effect.
CN102657673A Kalii dehydrographolidi succinas freeze-dried powder compound for injection and preparation method thereof The invention discloses a kalii dehydrographolidi succinas freeze-dried powder compound for injection and a preparation method thereof and relates to the field of medicines. The compound comprises the following active ingredients: 0.1%-99.9% of kalii dehydrographolidi succinas and 99.9%-0.1% of ribavirin. The preparation method of the freeze-dried powder compound for injection comprises the following specific operation steps: directly adding prescription doses of kalii dehydrographolidi succinas and ribavirin and 0.1-50% of another active ingredient such as sodium bicarbonate in water for injection; adding 0.1% of activated carbon and mixing for 30 minutes; adjusting the pH value to 6.5-6.7; then carrying out decarburization circulating filtration through a titanium rod for 30 minutes; afterwards, carrying out degerming circulating filtration through a 0.45 mu m of filter and a 0.22 mu m of filter for 30 minutes; sampling for inspection, filling after the sample meets the requirements and determining filling volume; after filling volume difference is qualified, half-buckling a butyl rubber plug for freeze-drying and putting the product in a freeze-drying box; and after freeze-drying is completed, obtaining the kalii dehydrographolidi succinas freeze-dried powder compound for injection. The preparation method disclosed by the invention has the advantages of being convenient in liquid processing, simplifying the aseptic operation process, improving the stability of the preparation, removing moisture in the product without thermal treatment, and enhancing the reconstitution property (dissolubility) of the preparation.
US20100184842 Ultraconserved Regions Encoding ncRNAs Described herein are methods for differentiate human cancers comprising using one or more transcribed ultraconserved regions (T-UCR) expression profiles where the association between the genomic location of UCRs and the analyzed cancer-related genomic elements is highly statistically significant and comparable to that reported for miRNAs.
US20110217384 Modified Release Dosage Forms of Skeletal Muscle Relaxants A unit dosage form, such as a capsule or the like, for delivering a skeletal muscle relaxant, such as cyclobenzaprine hydrochloride, into the body in an extended or sustained release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed. At least one bead population exhibits a pre-designed sustained release profile. Such a drug delivery system is designed for once-daily oral administration to maintain an adequate plasma concentration—time profile, thereby providing relief of muscle spasm associated with painful musculoskeletal conditions over a 24 hour period.
CN103610642A Lipidosome encapsulating epigallocatechin gallate and preparation method thereof The invention discloses a lipidosome encapsulating epigallocatechin gallate and a preparation method process. The lipidosome consists of the following components: soya bean lecithin, cholesterol, epigallocatechin gallate, buffer liquor and tween-80. The preparation method disclosed by the invention is simple in process and the EGCG lipidosome is prepared by a reverse evaporation method, and ultrasonic treatment is carried out on the lipidosome by a water bath ultrasonic instrument till the system is stable. The method can remarkably improve the stability of the EGCG lipidosome, and the grain size of the lipidosome can be effectively controlled and the encapsulation efficiency can be effectively improved by adjusting the ratio of the lipid components and the buffer liquor through the technical steps such as magnetic stirring, ultrasonic treatment and rotary evaporation. The EGCG lipidosome disclosed by the invention develops the application range of lipidosome, and the lipidosome is used as a carrier to encapsulate EGCG, so that the lipidosome is simple in preparation process, lower in demand on equipment, convenient to popularize and apply and can be industrially produced.
US20060058310 Remedies for vertebral canal stenosis The present invention relates to a preventive and/or therapeutic agent for spinal canal stenosis comprising aldose reductase inhibitory compounds. A representative example of aldose reductase inhibitory compounds is the compound represented by formula (I): wherein all the symbols represent the same meaning as described in the specification; a salt of its acid when R3a represents hydrogen, or solvate thereof The therapeutic agent of the present invention is effective for prevention and/or therapy for spinal canal stenosis and the like, such as lumbar spinal canal stenosis.
WO2007084591A2 Novel solid forms of (4r)-1-[4-(2-chloro-5-fluorobenzoyl)amino-3-methoxybenzoyl]-1,2,3,5-tetrahydro-spiro[4h-1-benzazepine-4,1'-[2]cyclopentene]-3'-carboxylic acid The present invention relates to novel solid forms of (4R)-1-[4-(2-chloro-5-fluorobenzoyl)amino-3-methoxybenzoyl]-1,2,3,5-tetrahydro-spiro[4H-1-benzazepine-4,1'-[2]cyclopentene]-3'-carboxylic acid (formula (I)) useful for treating and/or preventing conditions such as diabetic nephropathy, renal disease, renal failure and congestive heart failure.
CN1560064A Derivative of vibothymidine and its preparation process and application The invention discloses a thymine nucleoside derivative and its preparing method and its application, a compound which can be 3'-azidothymidine-5'-phosphorylated(N-methyl imidazole-2- formyl alkyl diamine) cyclohexyl ester and 2', 3'-dehydro and deoxy thymidine-5'-phsporylated (N-methyl imidazole-2- formyl alkyl diamine). It also provides its preparing method. The derivative is a candidate premedical compound with the effects of antivirus, antitumor and anti AIDS virus.
US6914072 E.g., ajulemic acid; used for decreasing cell proliferation The invention relates to the use of cannabinoid compounds (derivatives of tetrahydrocannabinol) for decreasing cell proliferation in a mammal.
WO2007024008A1 Preventive or therapeutic agent for side effect based on cytotoxicity of anticancer therapy containing apoptosis inhibition activity-enhancing protein fnk or nucleic acid encoding the same It is intended to provide a preventive or therapeutic agent for a side effect based on the cytotoxicity of anticancer therapy containing apoptosis inhibition activity-enhancing protein FNK or a nucleic acid encoding the same. The preventive or therapeutic agent for a side effect based on the cytotoxicity of anticancer therapy containing, as an active ingredient, FNK protein, in which at least one replacement selected from the replacement of Tyr-22 with Phe, the replacement of Gln-26 with Asn and the replacement of Arg-165 with Lys in Bcl-xL protein is contained, or a nucleic acid encoding the same.
CN103271892A Genistein positive ion nano lipid carrier and preparation method thereof The invention discloses a genistein positive ion nano lipid carrier and a preparation method thereof. Every 100ml of nano lipid carrier comprises the following components: 0.01-0.1g of genistein, 0.8-1.5g of solid lipid material, 0.5-1g of liquid lipid material, 0.1-0.2g of PEG (polyethylene glycol) modified liquid lipid material, 2-4g of emulsifier, 0.1-1g of copolymer of methacrylic acid and methacrylate and the balance of water. The prepared genistein positive ion nano lipid carrier is round in appearance and uniform in mass, encapsulation efficiency is more than 85%, and biocompatibility and biodegradability are good. By adopting the genistein positive ion nano lipid carrier, solubility of genistein is improved, in vitro release of genistein is prolonged, and the aims of prolonging intraocular preparation retention time and reducing toxic and side effects of a medicine are achieved.
CN103304502A Anti-diabetic compound, as well as preparation method and application thereof The invention relates to the field of medicines which are related to diabetes. Specifically, the invention relates to a compound containing an adamantane tetranitrazoleacetic acid structure, which is as shown in a general formula I, has a treatment effect against the diabetes and is used as a peroxisome proliferator-activated receptor (PPAR) agonist, as well as a preparation method and an application in the aspect of treating the diabetes, wherein the groups are as defined in the specification.
US20090221565 8-Fluoro-3-methyl-6-oxo-9-[(R)-3-(thiazol-2-ylamino)-pyrrolidin-1-yl]-2,3-dihydro-6H-1-oxa-3,3a-diaza-phenalene-5-carboxylic acid; can be solid or liquid A subject of the invention is the compounds of formula (I): in which either R1 represents H, OH, NH2, —(CH2)m—NRaRb(m=0.1 or 2), Ra and Rb represent H, linear, branched or cyclic (C1 -C6) alkyl, (C3-C6) cycloalkyl-(C3-C6)— alkyl, Rc, S(O)2Rc, C(O)Rc, S(O)2Rd or C(O)Rd; or Ra and Rb with N form an Rc radical; Rc represents a saturated, unsaturated or 5- or 6-members aromatic ring, containing 1 to 4 heteroatoms chosen from N, O and S, optionally substituted; Rd represents a linear, branched or cyclic (C1-C6) alkyl, optionally substituted by 1 to 4 halogens; or R1 represents Rc or CHReRc or CHReRd; Re represents H, OH, NH2, NH—(C1-C6)-alk or N-(C1-C6)-alk2, or NH—(C1-C7)-acyl or NHRc; R2 represents H, (CH2)m—NRaRb, Rc, CHReRc or CHReRd, and R′2 represents H; it being understood that R1 and R2 cannot at the same time be H or that R1 and R2 or R2 and R1 cannot be one (CH2)m—NRaRb or Rc or H and the other one OH, or one H and the other one NH2, or one H and the other one (CH2)m—NRaRb in which Ra and Rb represent H or alkyl or C(O)Rd, in which Rd represents an unsubstituted alkyl or cycloalkyl; or R1 has the above definition except H and R2 and R′2 together represent gem dialkyl or alkyl-oxime, or R2 and R′2 represent respectively Rc or Rd and OH, NH2, NHRc or NHRf, Rf being a (C1-C7) acyl radical; or R1 represents H and R2 and R′2 together represent alkyl-oxime or one represents Rc and the other one represents OH, NH2, NHRc or NHRf; n is 0 or 1; R3 and R′3 represent H or (C1-C6) alkyl optionally substituted by 1 to 3 halogens or R3 represents (C1-C6) alkoxy carbonyl and R′3 represents H; R4 represents methyl optionally substituted by halogen; R5 represents H, (C1-C6) alkyl or (C7-C12) arylalkyl; R6 represents H, fluorine, NO2, CF3 or CN; in the form of enantiomers or mixtures, as well as their salts with acids and bases; their preparation and their application as anti-bacterials, in both human and veterinary medicine.
WO2008139263A3 Methods for slowing the progression of multiple sclerosis Methods are provided herein for slowing the progression of multiple sclerosis comprising administering a therapeutically effective amount of a cannabinoid to a patient suffering from MS.
WO2010017570A2 Pharmaceutical form comprising tetrahydrobiopterin The invention relates to a pharmaceutical form comprising tetrahydrobiopterin or a metabolic precursor thereof, comprising an aqueous solution of tetrahydrobiopterin or a metabolic precursor thereof and an antioxidant in a dispensing container, and to a metering device for the metered dispensing of the aqueous solution, and further to the use of an antioxidant for stabilizing an aqueous solution of tetrahydrobiopterin, or a metabolic precursor thereof, for a storage period of at least one month.
CN1568978B Composition for preventing and treating whelk The invention relates to a composition for preventing and treating whelk, in particular the composition for preventing and treating acne / pimple.
CN102702200A (6RS)-5-methyl tetrahydrofolate calcium salt crystal form and preparation process thereof The invention discloses a (6RS)-5-methyl tetrahydrofolate calcium salt crystal form and a preparation process thereof. Diffraction peaks are generated in an X-ray diffraction pattern of the (6RS)-5-methyl tetrahydrofolate calcium salt crystal form when the 2theta angle is equal to 9.2+/-0.2, 15.0+/-0.2, 15.6+/-0.2, 21.1+/-0.2, 23.3+/-0.2, 27.2+/-0.2 and 28.6+/-0.2. The (6RS)-5-methyl tetrahydrofolate calcium salt crystal form has the advantages of high stability, purity and reproducibility, higher adaptability to industrial preparation in scale, and the like.
US20100292273 Cannabinoid Receptor Modulators Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*. and —CH2—O—C(R10)(R11)—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R3 is hydrogen, (C1-C)alkyl or (C1C3)fluoroalkyl; R4 is a radical of formula -(Alk1)p-(Q1)r (L)s-Q2 wherein p, r, s, Alk1, L, Q1 and Q2 are as specified; or R3and R4 taken together with the nitrogen to which they are attached form a cyclic amino ring of 4 to 7 ring atoms which is optionally substituted by a radical of formula -(L)s-Q2 wherein s, L and Q2 are as defined above, or by an optional substituent selected from hydroxy, methoxy, —NH2—, or mono- or di-(C1C3)alkylamino; R5, R6, R7 and R8 are each independently selected from hydrogen —F, —Cl, —Br, —CN, (C1-C3)alkyl, (C1C3)fluoroalkyl, cyclopropyl, and —OR9; R10 is hydrogen, (C1C3)alkyl, hydroxyl or NH2, and R11 is hydrogen or (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.
WO2013074633A1 Uracil derivatives as axl and c-met kinase inhibitors The present invention provides compounds of Formula I, or pharmaceutically acceptable salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c,Y, R3, X, E and G are as defined herein, methods of treatment and uses thereof.
WO2011149862A1 Nicotinic receptor non-competitive antagonists modulators The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.
CN102872354A Application of composition Xiaoke pills in preparation of information intervention agent, preparation method of information intervention body and product The invention relates to application of composition Xiaoke pills to preparation of an information intervention agent, a preparation method of an information intervention body and a product . The composition Xiaoke pills achieve an intervention effect by performing the reaction on Xiaoke pill information and a human body information receptor and adopting a Xiaoke pill information physical method without being used as a plant chemical treatment medicament. Therefore, after the Xiaoke pills are used as the information intervention body, the Xiaoke pill material is not consumed for the information intervention, so that the quality of the Xiaoke pills is not influenced and the Xiaoke pills also can be effectively reused as a plant chemical treatment conventional preparation.
US20060004028 Novel PARP inhibitor A compound represented by: or a salt thereof, and a pharmaceutical composition containing the compound or the salt, the compound having a poly (ADP-ribose)polymerase inhibitory effect, and is safe and advantageous for drug formulation.
CA2833912A1 Aav-based treatment of cholesterol-related disorders The invention in some aspects relates to methods and compositions for assessing the effectiveness of miRNA inhibitors. In other aspects of the invention, methods and compositions for treating cholesterol related disorders are provided. In one aspect of the invention, miRNA inhibitors against miR-122 and rAAV-based compositions comprising the same are provided.
WO2014080285A2 Pharmaceutical compositions having improved storage stability The present invention relates to a pharmaceutical composition that provides long-term stability of a hydrolytically labile antipsychotic agent
US20100137447 Method for the production of adsorbates of a rasagiline salt having a water-soluble adjuvant The present invention relates to an adsorbate of a pharmaceutically compatible rasagiline salt comprising at least one pharmaceutically compatible adjuvant, wherein the at least one pharmaceutically compatible adjuvant is a water-soluble, organic solvent and the rasagiline salt is present in the adsorbate as an amorphous substance.
WO2014114578A1 Pyrrolidine derivatives, pharmaceutical compositions and uses thereof The invention relates to new pyrrolidine derivatives of the formula (I), to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
WO2006106888A1 Oral composition for promoting defecation containing patchouli oil and dietary fiber [PROBLEMS] To provide an oral composition which promotes defecation and lessens abdominal distension. [MEANS FOR SOLVING PROBLEMS] By using an oral composition containing patchouli oil and a dietary fiber, the defecation frequency of a subject with a tendency toward constipation can be increased while a decrease in the defecation frequency of a normal subject with no tendency toward constipation can be regulated (i.e., the normal defecation frequency can be sustained and constipation can be prevented) and abdominal distension can be lessened owing to the dietary fiber. Examples of the dietary fiber include water-soluble dietary fibers such as guar gum, locust bean gum, tamarind gum, tara gum, xanthan gum, glucomannan, carrageenan, alginic acid or its salts, pectin, collagen, polydextrose, pullulan, acacia and carboxymethylcellulose sodium and insoluble dietary fibers such as cellulose, lignin, chitin, chitosan, hemicellulose, α-cellulose, microcrystalline cellulose, carboxymethylcellulose, methylcellulose, hydroxymethylcellulose and hydroxyethylcellulose.
US20090269390 Medical devices, polymers, compositions, and methods for delivering a haloacetate Polymers, compositions, and medical devices useful for delivering (e.g., by local and/or sustained delivery) a haloacetate (e.g., dichoroacetate) to a tissue are disclosed herein. Such methods can be useful for treatment of diseases such as cancer.
CN103356782A Drug for curing burn injury The invention relates to a drug for curing burn injury. The drug is prepared from gypsum, borneol, phellodendron, garden burnet, rosin, rheum officinale, stalactite, polygonum cuspidatum, and sophora flavescens. The drug for curing burn injury has the advantages of good cure effect, quick pain-killing effect, scar resistance, strong antibacterial effect, no toxic or side effects, and promotion on recovery of wounds.
WO2014155135A1 Methods for the treatment of autoimmune diseases The present invention provides a method for inducing CD8+FOXP3+ regulatory T cells in a subject which comprises administering to the subject: (i) a first agent which inhibits p38 phosphorylation; and (ii) a second agent which stimulates T-cell receptor (TCR) signalling. The method may be used to treat and/or prevent an autoimmune and/or inflammatory disease in a subject. The invention also provides compositions and kits for use in such methods.
US20080300274 Novel Pyrrolidino-1,4-Naphthoquinone Deriviatives and their Use for Treating Malignancies and Cardiovascular Diseases The invention provides pyrrolidino-substituted 1,4-naphthoquinone derivatives that modulate the activity of protein kinases, and it relates to the use of the derivatives in pharmaceutical compositions for treating cardiovascular disorders and malignancies. The invention particularly provides medicaments for treating disorders associated with MAPKs signaling, ERKs signaling, p38 signaling, and JNKs signaling.
CN102093258A Aromatic diamidine compound and synthesis method thereof The invention relates to an aromatic diamidine compound and a synthesis method thereof. The aromatic diamidine compound has the following structure, wherein R is an alkyl group or hydrogen. The synthesis method comprises the following steps: carrying out nitrile alcoholysis reaction on aromatic dinitrile used as the raw material and alcohol; introducing ammonia or amine to carry out alkoxy substitution reaction, thereby obtaining a saturated water solution of the crude product; properly adding excessive sodium hydroxide solution to the saturated water solution of the crude product, and vigorously stirring at low temperature until a great deal of solid precipitates; and filtering, washing with cold water, drying the solid, and purifying by recrystallization to obtain the aromatic diamidine compound. The aromatic diamidine compound provided by the invention has a novel chemical structure and unique chemical properties, can interact with biomacromolecules to be applied to the field of medicines, especially has the anti-tumor potential, and is hopeful to be converted into an important pharmaceutical intermediate. In addition, the synthesis method of the aromatic diamidine compound has the advantages of convenience, high efficiency, low cost, high yield (higher than 60%) and high purity (up to 98%), and is easy to implement.
US20120308601 Methods and materials for treating cancer This document provides methods and materials related to treating cancer. For example, methods and materials for using nucleic acid libraries to treat cancer are provided.
US7312342 Process for the preparation of (3-cyano-1h-indol-7-yl) (4-(4-fluorophenethyl) piperazin-1-yl)-methanone and salts thereof The present invention relates to a process for the preparation of (3-cyano-1H-indol-7-yl)[4-(4-fluorophenethyl)piperazin-1-yl]-methanone and salts thereof, characterised in that an indole ester of the formula II in which R is as defined in Claim 1, is converter into 3-cyano-1H-indole-7-carboxylic acid via steps (1) to (4) according to Claim 1, and this is reacted with 1-[2-(4-fluorophenyl)ethyl]piperazine of salts thereof to give the product.
WO2012167434A1 A pharmaceutical composition for inhibiting recurrence, aggravation and metastasis of hepatocarcinoma A pharmaceutical composition for inhibiting recurrence, aggravation and metastasis of hepatocarcinoma comprising at lease one compounds represented by formula (I) and pharmaceutically acceptable carriers.
EP2675803A1 Macrocyclic integrase inhibitors for use in the treatment of feline immunodeficiency virus This invention concerns to naphthyridin derivatives of formula (I) for use in the treatment or prevention of feline immunodeficiency virus (FIV). Furthermore the present invention relates to a method of treating or preventing infection of feline immunodeficiency virus in a feline animal wherein said method comprises the administration to said feline animal of a therapeutically effective amount of a naphthyridin derivative.
CN1714795A Eye drop and its preparing method and use The present invention belongs to the field of medicine technology, relates to one kind of eye drop, and is especially one kind of eye drop for treating xerophthalmia, blepharitis, tarsal gland dysfunction and other eye surface inflammations and its preparation process and use. The eye drop contains osmotic buffering agent, distilled water, and vibramycin hydrochloride. The preparation process includes the following steps: dissolving vibramycin hydrochloride and osmotic buffering agent in distilled water; adding distilled water to required volume and regulating pH to 5.5-6.0; membrane filtering to sterilize and packing. Or, the eye drop is prepared through preparing abacterial vibramycin hydrochloride powder; dissolving osmotic buffering agent in distilled water and regulating pH to 5.5-6.0; membrane filtering to sterilize and dissolving vibramycin hydrochloride powder in the distilled water solution.
CN1965885A Application of total flavones of chickpea in preparation of medicament for treating diabetes The invention relates to an application of chick-pea flavone in antidiabetic, wherein said production comprises that: using ligarine to degrease chick-pea, drying, using alcohol to extract, dissolving the paste in hot water, adjusting pH to 9-11, eccentrically filtering, taking out upper clear liquid, separating said clear liquid via porous resin post, using 20-60% alcohol solution to wash, collecting the part with high flavone content, evaporating solvent, to obtain the final product whose flavone content is higher than 50%. The inventive method has simple process and low cost.
CN102058607A Medicament for treating onychomycosis (tinea manus and tinea pedis) The invention relates to a medicament for treating onychomycosis (tinea manus and tinea pedis). The medicament is characterized by comprising the following components in part by weight: 100 parts of cosmetic base stock, 25 to 40 parts of urea and 15 to 30 parts of salicylic acid. The medicament has the advantages that: compared with the current similar medicament, the medicament has the advantages of short course of treatment, quick response, convenience of use, and no pains; repeated clinical demonstration for many years proves that the medicament has reliable curative effect, no toxic or side effect, and remarkable seepage force, can directly, rapidly and thoroughly kill fungi and bacteria on the skin and deep in the skin, and can achieve treatment effect in a short time.
EP1100507B1 Use of a combination comprising a precursor of uric acid and antioxidant for the treatment of neurodegenerative deseases Damage to cells, tissue and other body parts in a mammalian host may be treated by using hypoxanthine and in conjunction with at least one biological modifier, which may be a free radical scavenger or a metabolic inhibitor. The biological modifier is preferably uric acid, buthionine sulphoximine, vitamin C, aspirin, or nordihydroguaiaretic acid. Such a combination may be used to treat, for example, cancer, infectious diseases, neurodegenerative disease and damage caused by radiation therapy, high oxygen tension, and chemotherapy.
CN1990452A Process to produce a protease inhibitor Disclosed is a novel process and novel intermediates to prepare [R-(R*,R*) ]-N-[3-[1-[5, 6-dihydro-4-hydroxy -2-oxo-6-(2-phenylethyl) -6-propyl-2H-pyran-3- yl]propyl]phenyl]-5- (trifluoromethyl)-2- pyridinesulfonamide (XIX) which is a protease inhibitor useful in treating humans infected with the HIV virus.
CN103356662A Injection tigecycline composition and preparation method thereof The invention provides a stable injection tigecycline composition and a preparation method thereof. The tigecycline composition comprises the following components in parts by weight: 10 parts of tigecycline, 5 to 50 parts of at least one carbohydrate and 0.25 to 10 parts of sodium salt, wherein the pH value of the injection tigecycline composition is 3.5-6.5. According to the injection tigecycline composition, the stability of the tigecyline solution and solid state can be greatly improved. The preparation process is simple and controllable, and the product quality is stable, so that considerable economic and social benefits can be produced.
WO2008138383A1 Method for the production of n-methyl naltrexone bromide The invention relates to a method for the production of n-methyl naltrexone bromide, wherein a compound of the general formula (I), in which X- represents an anion that is different from a bromide anion and R represents hydrogen or a nucleofuge, (i) is dissolved or dispersed in a suitable polar solvent, (ii) said solution or dispersion is mixed with a compound containing bromide anions, and (iii) the reaction mixture thus obtained is stirred until the n-methyl naltrexone bromide has formed and crystallized, wherein, (iv) if R represents a nucleofuge, R is removed before, during, or after the conversion.
CN102716099A Levocetirizine hydrochloride chewable tablet and preparation method thereof The invention relates to a levocetirizine hydrochloride chewable tablet for relieving hypersensitivity caused by allergy diseases and the preparation technology thereof. Levocetirizine hydrochloride has stronger bitterness, in the invention, by adopting the composite of Beta-cyclodextrin and microcrystalline cellulose, the medicine is prepared to be inclusion compound so as to cover up the bitterness of the medicine, the prepared medicine is better in mouth-feel and is convenient to take, the process operability in preparing the inclusion compound and the stability of the levocetirizine hydrochloride chewable tablet are enhanced at the same time, the levocetirizine hydrochloride chewable tablet is particularly suitable for old and child patients having difficulty in swallowing, enhances the compliance of the patients and has a better marketable value.
WO2007015002A2 Novel crystalline iv form of agomelatine, method of the preparation thereof and pharmaceutical compositions containing said form The crystalline form IV of a compound of formula (I) is characterised by the X diffraction diagram thereof on a powder.
US7803823 having proinflammatory cytokine production inhibiting properties, in particular tumor necrosis factor-alpha (TNF-alpha) and/or interleukin-12 (IL-12) inhibiting properties, used for the prevention or the treatment of inflammatory and/or autoimmune diseases This invention concerns the use of a compound of formula (I′) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono- or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula L is optionally substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of inflammatory and/or auto-immune diseases mediated through TNF-α and/or IL-12.
CN103429234A Use of jasmonate to treat bladder dysfunction A formulation or composition contractility comprising jasmonate for modulating bladder and/or treating bladder dysfunction, particularly an overactive bladder in a mammal, particularly a human and use of jasmonate for treating bladder dysfunction is provided.
US20110150968 Dissolvable dietary supplement strip and methods for using the same A strip, which is both edible and dissolvable, is provided comprising a film and a dosage of at least 2% of the reference daily intake (RDI) of at least one dietary supplement for malnutrition or to prevent/treat alcohol induced hangovers. A method for treating malnutrition and/or preventing and treating alcohol-induced hangovers using a dissolvable orally administered strip.
WO2014068265A1 Antiviral phosphonate analogues and process for preparation thereof The present invention provides a compound of the Formula (I) wherein R is 9-isopropyl-9H-purin-6-amine; 2-amino-9-isopropyl-lH-purin-6(9H)-one; 4-amino- 1-isopropyl pyrimidin-2(lH)-one; or l-isopropyl-5-methyIpyrimidine-2,4(lH,3H)-dione, R' is - CH2OC(0)R", and R" is -C(CH3)3 or -CH(CH3)2 including pharmaceutically acceptable salts thereof. The present invention also provides a process for preparing a compound of formula (la) and a compound of formula (I) for use in treating a viral infection.
US7094804 Water free ubiquinone concentrate A water soluble, essentially water-free ubichinon concentrate is described, which contains an emulsifier with an HLB value between 9 and 16, ubichinon Q10, as well as a light oil containing triglyceride. Furthermore, a method for producing the concentrate is described.
WO2014141847A1 Therapeutic agent for systemic bone disease and use thereof The present invention addresses the problem of providing a novel therapeutic strategy which has excellent therapeutic effects on systemic bone diseases caused by over-activation of FGFR3, in particular, achondroplasia and hypochondroplasia. A therapeutic agent for systemic bone disease is provided which comprises, as an active ingredient, meclizine or a pharmaceutically acceptable salt thereof.
US20050026926 N, N'-disubstituted piperazine compounds and their use as analgesics N,N′-disubstituted piperazine compounds, processes for the production thereof, and pharmaceutical preparations containing these compounds. The use of N,N′-disubstituted piperazine compounds for the production of pharmaceutical preparations and in related methods of treatment.
US7045516 Irritable bowel diosrders; gastrointestinal disorders; diarrhea A compound represented by the following general formula (1): wherein R1 represents a halogen atom, R2 represents hydrogen atom or a lower alkyl group, and R3 represents hydrogen atom, a lower alkyl group, a lower alkoxyl group, a hydroxy lower alkyl group, a halogen atom, or a substituted or unsubstituted amino group, wherein a substituent on the amino group is selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkylcarbonyl group, and an amino protective group, or a salt thereof. The compound of the present invention or a salt thereof is useful as an active ingredient of medicaments for preventive and/or therapeutic treatment of conditions of irritable bowel syndrome and digestive tract functional disorder, or condition of diarrhea.
US20100069346 New Azetidine Derivatives as Neurokinin Receptor Antagonists for the Treatment of Gastrointestinal Diseases The application relates to new piperazine- or morpholine-substituted azetidine derivatives of formula I. These compounds are antagonists at the neurokinin receptor and can be used for the treatment of gastrointestinal diseases. The application also relates to processes for the preparation of the compounds and to intermediates in said preparation.
CN102641269A Application of bulleyaconitine to prepare medicament capable of suppressing pathological pain caused by paclitaxel chemotherapy medicament The invention relates to application of bulleyaconitine to prepare a medicament capable of suppressing pathological pain caused by paclitaxel chemotherapy medicaments, which belongs to the technical field of medicaments, in particular to application of bulleyaconitine to analgesic medicaments. The bulleyaconitine provided by the invention has a prevention or treatment effect on the pathological pain caused by the paclitaxel chemotherapy medicaments, and the suppressing effects are different in different concentrations. When the suppressing effects are applied to chemotherapy, the pain of a patient can be reduced. The bulleyaconitine has a favorable application prospect.
CN101961338A Anti-tumor medicine composition The invention relates to an anti-tumor medicine composition, comprising a compound cyclosuffrobuxinine M with a therapeutically effective amount shown as a general formula (FORMULA), and a pharmaceutically acceptable carrier. The invention also relates to a preparation method of the anti-tumor medicine composition and application of preparing anti-tumor medicines thereof.
CN103446159A Pharmaceutical composition containing pediatric compound amino acid injection and cefotiam hydrochloride The invention relates to a pharmaceutical composition containing cefotiam hydrochloride and pediatric compound amino acid injection (19AA-I), and in particular relates to a combined application package, comprising cefotiam hydrochloride for injection and pediatric compound amino acid injection (19AA-I). Compared with the combined and mixed application of the two medicines, the combined application package has the advantages that the steps are simplified and the safety of the medication in children is improved, furthermore, the combined application package is very good for the stability of the cefotiam hydrochloride, therefore the clinic application quality and the bioavailability of the drug are enhanced.
CN1839859A Ginsenoside F1 medicinal uses Disclosed is the use of Ginsenoside F1 in preparing medicament for the treatment of regenerative anemia.
CN101428144A Polysaccharide combined vaccine for epidemic encephalitis and preparation method thereof The invention provides an epidemic meningitis polysaccharide combined vaccine, and aims to prepare a freeze-dried ACYW135 meningococcal polysaccharide vaccine by the process of removing endotoxins by the ultracentrifugation method so as to ensure that the content of endotoxins present in ACYW135 group meningococcal polysaccharide stock solution is far lower than that before the centrifugation. The vaccine provided by the invention has the advantages of ensuring that only one injection is enough to prevent a patient from being infected with epidemic meningitis disease, achieving, if not greater, as much preventive effect as four injections initially, alleviating the suffering of the patient, and reducing the prevention cost.
US20080027099 Bicyclic heteroaryl inhibitors of pde4 The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.
EP2572712A2 Treatment of viral infections by modulation of host cell metabolic pathways Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in "suicide" of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models.; Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.
US20110053943 CARBAMATE AND UREA INHIBITORS OF 11ß-HYDROXYSTEROID DEHYDROGENASE 1 This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
US20110124634 Bioactive compounds for treatment of cancer and neurodegenerative diseases The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.
CA2279939C Treatment and prevention of adhesions An inhibitor of adhesion formation which can be used to prevent adhesions within the abdominal cavity, particularly following surgical intervention in the area. Specifically, the most preferred compound of the present invention, Halofuginone, can be used to prevent collagen deposition from occurring within the peritoneum after such surgical intervention, thereby inhibiting adhesion formation. Halofuginone, and related compounds, are useful in the prevention and treatment of both inflammatory and surgically induced adhesions, and in the treatment of congenital adhesions.
CN102935076A Capsule containing atorvastatin sodium and preparation method thereof The invention relates to a capsule containing atorvastatin sodium and a preparation method thereof, wherein the capsule containing atorvastatin sodium is used for treating patients with primary hypercholesterolemia and mixed hyperlipemia. The main component of the capsule is amorphous atorvastatin sodium crude drug, and the amorphous atorvastatin sodium crude drug is prepared into particles or powder or particles and powder by using one or multiple auxiliary materials, and then is filled into a stomach-dissolving type hollow capsule. The preparation method is simple, content of basic remedy of the medicine is stable, and the medicine is quick in disintegration and good in dissolution rate.
CN102229611A 2,6-diaryl pyrazolo[1,5-a]pyrazine-4(5H)-ketone compound and its application The invention discloses a 5-substituted ethylene-2,6-diaryl pyrazolo[1,5-A]pyrazine-4(5H)-ketone derivative and its application in the preparation of antitumor drugs. Experimental results show that the compound provided by the invention has a remarkable effect of inhibiting the propagation of lung cancer cells and has a better inhibitory activity against lung cancer A549 than its inhibitory activity against H322; in addition, the inhibitory activity of the compound displays a dose dependency; it is indicated that the novel pyrazoles derivative has a prospect of clinic application and development.
WO2005087787A1 2-fluoro-6-o-substituted ketolide derivative The 2-fluoro-6-O-substituted ketolide derivative represented by the formula [Chemical formula 1] (1) or a pharmaceutically acceptable salt or hydrate thereof. They are new erythromycin derivatives which have potent antibacterial activity against erythromycin-resistant pneumococci or erythromycin-resistant streptococci and are reduced in drug interaction.
WO2012126472A1 Gaba-c receptor agonists or antagonists for use in the treatment of vascular diseases The present invention relates to novel methods for regulation of blood flow, which may be used in particular in the treatment of retinal disorders that involve constriction or dilation of the retinal arterioles.
CN101590047A Pharmaceutical composition containing amlodipine and epristeride The invention discloses a pharmaceutical composition containing amlodipine, epristeride and a pharmaceutically acceptable carrier, and application of the pharmaceutical composition in preparing medicines for treating the diseases concerning benign prostatic hyperplasia (BPH). With the implementation of the invention, the pharmaceutical composition with special usage, provided to the patients, not only has precise curative effect but also can improve compliance of the patients, bring convenience to the patients to take medicines and reduce medical expenses, thus enjoying good market prospect.
CN1694715B Use of beta glucan particles and antibodies in preparing medicine for cancer therapy The present invention relates to methods of using neutral soluble glucan and monoclonal antibodies for antitumor therapy. Neutral soluble Beta (1,3; 1,6) glucan (NSG) enhances the tumoricidal activity of the innate immune system by binding to the C3 complement protein receptor CR3. The glucan does not stimulate the induction of inflammatory cytokines. Also described are methods of using whole glucan particles (WGP) as an immunomodulator by inducing a shift from a Th2 response to the Thl response, leading to an enhanced antitumor cytotoxic T-cell response.
WO2010028011A1 Amides of diazabicyclononanes and uses thereof The present invention relates to compounds of the following formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
CA2623769A1 Composition and method for the prevention of oral disease The discovery of use of stabilized chlorine dioxide at a concentration range of about 0.5% to about 0.9% (w/v) as a composition for the prevention of oral disease through bactericidal and bacteriostatic properties within a microbial environment is disclosed. The bactericidal properties of stabilized chlorine dioxide are further expanded to include kill of an increased number of anaerobic/aerobic/facultative gram-negative and gram-positive oral bacteria occurring in mixed microbial communities. The further discovery of the bacteriostatic properties of stabilized chlorine dioxide present within a microbial environment which inhibit the re-growth rate of oral bacteria after exposure resulting in significant reduction of plaque and oral malodor production is disclosed. The stabilized chlorine dioxide may be in the form of an oral wash or rinse in solution.
US20100104618 Polymer-based surgically implantable haloperidol delivery systems and methods for their production and use Surgically implantable drug delivery systems for long-term delivery of haloperidol containing a biodegradable polymer and haloperidol fabricated into the surgically implantable drug delivery systems via solvent casting and compression molding are provided. Also provided are methods for producing the surgically implantable drug delivery systems and methods for using these systems in the treatment of psychotic disorders such as schizophrenia.
CN103446055A Preparation method for genistein lipid nano body The invention relates to a preparation method for a genistein lipid nano body. The preparation method comprises the operation steps of (1) dissolving cholesterol-hydrate and soybean lecithin into trichloromethane, evaporating in water bath at constant temperature rotatably, thereby obtaining a uniform film; (2) dissolving genistein into absolute alcohol, and then adding a PBS (phosphate buffer solution) to obtain genistein mixed liquor; (3) adding the genistein mixed liquor, three small glass beads and tween-80 into the uniform film, and washing the film in water bath at constant temperature rotatably; (4) carrying out water bath ultrasonic treatment, and sieving with a micropore filtering film; (5) freezing and drying the film to obtain genistein lipid nano body solids. The encapsulation efficiency is greater than 59.5 percent, and the drug loading capacity is greater than 17.45 percent; the genistein lipid nano-body solids are powdery solids with even particles; the average particle size of particles is 50-60nm; the particle size of 96 percent of liposome is within 100nm. The genistein lipid nano body improves the biological utilization rate of the genistein in vivo.
CN101693012A Preparation and application of florfenicol slowly-releasing micropill for treating animal digestive canal infection The invention relates to preparation and application of florfenicol slowly-releasing micropills for treating animal digestive canal infection. The implementation comprises the following steps: weighing drug accessories and florfenicol raw materials according to the proportion of weight ratio 0.1-10:1, preparing micropills whose grain size dimension is between 0.5 to 3mm, wrapping a non-pH dependency high molecular polymer film outside the micropills, wherein the film contains low molecular water-soluble materials. Slowly-releasing micropills containing florfenicol is wrapped by non-pH dependency high molecular polymer materials, water-soluble materials such as mannidex, antacidin or natrii chloridum are added in the wrapping film, after people take the wrapped micropill orally, the water-soluble component in the wrapping film is dissolved to form a pore passage, and the drug is slowly released from the pore passage and exerts the long-term curative effect in the intestinal tract. The drug is different from traditional drug feeding modes in that higher drug concentration can be kept in intestinal tracts for long time, directional distribution of the drug in the intestinal tract can lower the side effects of drug to other organs and tissues, and the treatment cost can be lowered due to less drug dosage.
US7494997 excellent BCR-ABL tyrosine kinase inhibitory activity; to treat leukemias; 3-bromo-4-(4-methylpiperazin-1-ylmethyl)-N-{4-methyl-3-[4-(3-pyridyl)pyrimidin-2-ylamino]phenyl}benzamide; compounds with cell growth inhibitory effect The present invention provides an amide derivative represented by the following general formula (1): wherein R1 represents a saturated cyclic amino group, R2 represents alkyl, halogen or haloalkyl, R3 represents hydrogen or halogen, Het 2 represents pyridyl or pyrimidinyl, and Het 1 represents a group of the formula [6], or a salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.
WO2006041843A3 Pharmaceutical dosage form comprising meloxicam Meloxicam powder having a mean particle size of about 2 µm to about 25 µm, pharmaceutical compositions containing the powder, a process to prepare the compositions, and their use in the treatment of conditions such as inflammation, pain, fever and arthritis.
CN103251573A Protein micro/nano sphere carrying antitumor chemotherapeutic medicine and preparation method of protein micro/nano sphere The invention relates to a protein micro/nano sphere carrying an antitumor chemotherapeutic medicine. The composition preferably comprises a housing and a core on the premise that the protein is TNFSF (Tumor Necrosis Factor Superfamily) protein, and the antitumor chemotherapeutic medicine is an indissolvable medicine; the housing is composed of the TNFSF protein and is basically completely closed; the core is placed into the housing and contains the antitumor chemotherapeutic medicine; and the maximum diameter of the housing is less than 500nm. The protein micro/nano sphere carrying the antitumor chemotherapeutic medicine has the beneficial effects that the protein micro/nano sphere which is prepared based on the membrane emulsification technology and can carry an indissolvable antitumor chemotherapeutic medicine is provided; and the invention particularly provides a preparation method of the protein micro/nano sphered of the TNFSF protein and HAS (Human Serum Albumin) protein, represented by TRAIL (Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand).
WO2009024361A1 Hair treatment compositions with alcohol(s) and melatonin/agomelatine Hair treatment compositions which impart advantageous properties to the hair treated with them and protect the hair against external influences comprise 0.1 to 90% by weight of at least one monohydric alcohol from the group ethanol, n-propanol, isoporopanol, n-butanol, 0 to 10% by weight of at least one gel former, 0.001 to 5% by weight of melatonin (I) and/or one of its salts and/or agomelatine (II) and/or one of its salts, and 0.001 to 5% by weight of at least one care enhancer from the group L-carnitine and/or its salts; panthenol; the 2-furanones, in particular pantolactone; taurine and/or its salts; vitamins, in particular niacinamide, biotin, pantothenic acid and tocopherol and/or derivatives thereof; ubiquinone; ectoin; allantoin; plant extracts in particular of echinacea or moringa plants; xanthines, in particular caffeine, theophylline and theobromine; flavonoids, in particular flavonols; bisabolol; creatine.
WO2013089168A1 Method for producing neuraminic acid derivative The present invention provides a method for producing a neuraminic acid derivative. A method for producing a compound represented by formula (I) [wherein R1 represents a C1-C19 alkyl group] or a pharmacologically acceptable salt thereof using N-acetylneuraminic acid dihydrate as a starting raw material.
US20080070836 Zinc transporter LIV1 can be used as an epithelial-mesenchymal transition (EMT) regulatory agent; further, because EMT is involved in cancer progression, LIV1 antisense nucleotides and the like may be used as pharmaceuticals for treating cancer The mechanism of STAT3, which is considered to play a crucial role in EMT, was elucidated using zebrafish embryos. Unexpectedly, a STAT3 target gene turned out to be zinc transporter LIV1. The present inventors studied the relationship between STAT3 and LIV1 in EMT, and further studied their relationship with zinc finger protein Snail, known for its association with EMT. The results showed that LIV1, whose expression is regulated by STAT3, activated Snail, thereby ultimately inducing EMT. LIV1 can be used as an EMT regulatory agent. Further, because EMT is involved in cancer progression, LIV1 antisense nucleotides and the like may be used as pharmaceuticals for treating cancer.
US7348429 Process for purifying N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide(zaleplon) and crystalline forms of zaleplon accessible with the process Provided are novel Zaleplon crystalline Forms II, III, IV and V, which are useful for the treatment of insomnia. Also provided are processes for making Forms I, II, and V using precipitation methods.
WO2007017096A1 Pyrazine derivatives useful as adenosine receptor antagonists The present invention provides a compound of formula (I) wherein: A represents an optionally substituted monocyclic or polycyclic aryl or heteroaryl group B represents an optionally substituted monocyclic nitrogen-containing heteroaryl group ; and either a) R1 and R2 represent hydrogen or specified substituents, or b) R2, R1 and the -NH- group to which R1 is attached, form a moiety selected from the moiety of formulae (IIa) and (IIb): (IIa) These compounds are useful as antagonists of the A2B receptor, for instance in the treatment of asthma.
EP1091735B1 Improved enriched platelet wound healant A wound healant composition comprising a therapeutically effective amount of activated growth factors and ascorbic acid and/or at least one retinoid and/or at least one antibiotic, that facilitates the growth of new tissue.
US20130005694 Liquid compositions comprising vitamin d and uses thereof The present invention relates to a liquid composition comprising vitamin D, or a salt thereof. Specific embodiments employ 5000 IU to 250,000 IU, and include sorbate and benzoate as a preserving agent.
WO2007009715A1 2-cyano-pyrimidines and -triazines as cysteine protease inhibitors The invention relates to compounds of the formula (I) and salts thereof, to a process for their manufacture, to their use in the treatment of (especially cysteine protease, such as UCH-L3- and/or USP-2 dependent) diseases or for the manufacture of pharmaceutical formulations against these diseases, methods of treatment of warm-blooded animals comprising administering the compounds and/or their salts to said animals and pharmaceutical preparations, especially for the treatment of the diseases, comprising said compounds and/or salts.
WO2005023289A1 Medicinal composition for treating chronic hepatitis c It is intended to provide a medicinal composition for treating chronic hepatitis C characterized by containing at least one active ingredient selected from the group consisting of IL-15, myeloid dendritic cell maturation stimulators (for example, CpG oligo deoxynucleotide, GM-CSF, IL-4, LPS, CD40L, polyI:C, TNF-α and IFN-Ϝ) and lectin-binding substances (for example, mannose carbohydrate, fucose carbohydrate and antilectin antibody); and a method of treating chronic hepatitis C by using such active ingredient(s). In the above medicinal composition and therapeutic method, it is possible to use IFN-α together with these active ingredients.
WO2014069846A1 Method for preparing 1-deoxy-1-(2-hydroxyethyl amino)-d-glucitol and miglitol The present invention relates to a method for preparing 1-deoxy-1-(2-hydroxyethyl amino)-D-glucitol from D-glucitol by using a borohydride complex as a reducing agent, and to a method for preparing miglitol from the 1-deoxy-1-(2-hydroxyethyl amino)-D-glucitol. The present invention has valuable use in the preparation of miglitol which is a therapeutic agent for diabetes.
WO2012106990A1 Chinese medicine fuming and washing agent for treating tinea capitis A Chinese medicine fuming and washing agent for treating tinea capitis, which is formulated using Chinese herbal medicine raw materials in the following weight proportions: 10-20 parts of radix sophorae flavescentis, 8-15 parts of Cinnamomum camphora root, 10-25 parts of capillary artemisia, 15-25 parts of Coptis chinensis, 15-25 parts of radix stemonae, 15-30 parts of liquorice, 15-30 parts of Symplocos sumuntia, 10-20 parts of Stellera chamaejasme, 10-20 parts of realgar, 15-25 parts of herba schizonepetae, 15-25 parts of Ledebouriella seseloides, 15-25 parts of Angelica polyclada, 15-25 parts of Lithospermum purpurocaeruleum, 15-30 parts of Angelica sinensis, 15-20 parts of Ligusticum wallichii, 8-15 parts of dandelion, 15-20 parts of cortex dictamni, 10-25 parts of Portulaca oleracea, 15-25 parts of fructus kochiae, and 5-10 parts of Lonicera japonica. The Chinese medicine fuming and washing agent of the present invention is convenient to use, has no toxic or side effects, and has the effect of killing bacteria, of resisting inflammation and allergies and of relieving itch; it can also increase the hydration of the cuticles and eliminate unbearable itch, redness and swelling caused by a local inflammation, and can dissolve keratin and increase proteins, so as to prevent skin keratinization and increase the penetrability and flexibility of the skin.
CN102178680B Long-acting and high-content Huperzine plaster and preparation method thereof The invention relates to a Huperzine paster and a preparation method thereof. The Huperzine paster is a flaky transdermal absorption preparation formed by overlapping an adhesive layer, a medicament substrate and a supporting layer, wherein the medicament layer comprises the Huperzine, pharmaceutically acceptable salt, lecithin and paster conventional auxiliary materials; the weight ratio of the lecithin to the Huperzine is 1:(0.4-2.5); the medicament substrate is coated on the adhesive layer and the coating thickness is 0.35 to 0.6 mm; and the pH value of the paster is between 5.0 and 8.0. The Huperzine paster is administrated through a transdermal penetration route, overcomes the defects of the original Huperzine paster, can be absorbed in a human body quickly, has long-term effectiveness and high content, solves the problem of high medicament residual ratio of the common paster, and is used for treating or preventing nerve system diseases such as Parkinson's disease, senile dementia, depression and the like.
CN101259201A Antirheumatic pain relieving medicaments A medicine for resisting rheumatism and alleviating pain is made from the materials with the following weight portions: 50 to 55 portions of gentian root, 70 to 75 portions of hemlock parsley, 70 to 75 portions of peach kernel, 65 to 70 portions of safflower, 50 to 60 portions of liquorice, 45 to 50 portions of notopterygium root, 60 to 65 portions of myrrh, 70 to 75 portions of angelica, 70 to 75 portions of boninrousette, 45 to 50 portions of nutgrass galingale rhizome, 75 to 80 portions of achyranthes root, 65 to 70 portions of earthworm, 65 to 70 portions of rhizoma atractylodis, 55 to 60 portions of corktree bark, 60 to 70 portions of milk veteh, 60 to 65 portions of salvia miltiorrhiza, 60 to 65 portions of spatholobus stem, 60 to 65 portions of pawpaw, 55 to 65 portions of paniculater swallowwort root, 60 to 65 portions of pachyma cocos, 55 to 60 portions of ground beetle, 40 to 45 portions of natural copper and 35 to 40 portions of dragon blood. The medicine can cure rheumatoid arthritis, hyperosteogeny, sciatica, cervical spondylosis, periarthritis, various arthralgia, neuralgia, kidney deficiency, lumbocrural pain, myalgia, exercise injury pain and lumbar disc protrusion, which is effective in treatment.
EP1648467A1 Process for preparing particles containing an antiviral A process for preparing a particle comprising a co-precipitate surrounding a neutral hydrophilic carrier, said process comprising spraying an organic solution on a neutral hydrophilic carrier, said solution comprising at least one triazine or pyrimidine active ingredient having HIV inhibiting properties, one surface active agent, and one hydrophilic polymer, wherein the spraying of whole of the solution occurs in at least two separate steps, each of these steps followed by a grinding step of the product obtained at the end of the preceding step.
US20050119261 Analgesics; neuropathic pain; antiepileptic agents; irritable bowel syndrome; antidepressants; anxiolytic agents; multiple sclerosis; bipolar disorders Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.
CN1817341A Solid sustained preparation of miglinon and its preparing method A slow-release solid of miglinar for treating the diabetes B is prepared from the miglinar (5-20%), slow-releasing retarder (5-50%) and medicinal additives (30-80%).
CN103566104A Medicinal liquor for alleviating toothache The invention provides medicinal liquor for alleviating toothache. The medicinal liquor comprises the following components by weight: 80g of dried rehmannia roots, 80g of radix angelicae pubescentis, 30g of asarum, 10g of crude sichuan aconite roots, 10g of raw kusnezoff monkshood roots, 10g of radix angelicae, 7.5g of Angelica sinensis, 7.5g of ubprocessed Rhizoma Pinelliae, 7.5g of flos daturae, 7.5g of raw Arisaema consanguineum Schott, 15g of fructus zanthoxyli and 500ml of 75% ethanol. The invention aims to provide the medicinal liquor for alleviating toothache. The medicinal liquor for alleviating toothache has the effect of alleviating pain by external use under a condition of midnight or inability of going to hospital due to unallowed condition. Besides anesthetization and pain-reliving, the medicinal liquor further has the effects of clearing away heat and toxic materials and diminishing inflammation.
US20100190827 treating diseases responsive to cannabinoid receptor antagonism; using particular crystallization conditions, a novel stable crystalline form called form II is obtained The present invention relates to a novel crystalline polymorph of rimonabant, its method of preparation and the pharmaceutical compositions containing this novel polymorph.
CN101503399B C-aryl glucoside SGLT2 inhibitor The invention relates to a C-aryl glucoside derivative indicated by a general formula I, as well as a usage and a composition thereof. The C-aryl glucoside derivative has a good effect in inhibiting SGLT. The composition can be separately used or used together with other antidiabetic medicine or other therapeutic agent and can be used for preventing or curing diabetes and other relevant diseases.
US20110046081 Classical cannabinoid metabolites and methods of use thereof The present invention encompasses classical cannabinoid metabolites and uses thereof.
US7960366 Substituted tetracycline compounds as synergistic antifungal agents Methods and compositions for treating for the synergistic treatment of fungal associated disorders are discussed.
US20130005677 2'-fluoro-6'-methylene carbocyclic nucleosides and methods of treating viral infections The present invention relates to 2′-Fluoro-6′-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.
WO2013107429A1 1-oxo/acylation-14-acylated oridonin derivative, preparation method therefor and application thereof The present invention relates to the fields of natural medicine and medicinal chemistry, and more particularly to a 1-oxo/acylation-14-acylated oridonin derivative of a general formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing the compounds, a pharmaceutical composition comprising the compounds, and application thereof in preparation of antitumor drugs.
CN101024014A Medicine composition for treating cough and asthma The present invention provides a medicine composition for curing cough and asthma. It is made up by using bitter apricot, crude gypsum, licorice extract powder, star anise oil, camphor, ephedrine hydrochloride, calcium carbonate, sodium benzoate, sulfamethoxazole, methoxybentine and theobromine through a certain preparation process. Said medicine has good therapeutic effect for curing cough, asthma and infection of respiratory tract.
CN1919222A Process for preparing notoginsen triterpenes The invention discloses a process for preparing Notoginsen triterpenes injection, which comprises steps of immersing notoginseng with water, charging cellulose for enzymolysis, watering extracted muck or charging 10-90% of ethanol for extraction, concentrating the extract and passing through anion exchange resin column, concentrating eluent into concrete through decompressing, finally drying.
CN101502653A Medicament composition for preventing or treating Streptococcus suis disease The invention discloses a medicine combination for preventing or treating streptococcosis suis, belonging to the prevention and control field of animal diseases. The medicine combination is composed of beta-monobactams antibiotics and macrolides antibiotics featuring effective dose in treatment; wherein, the beta-monobactams antibiotics is preferably amoxicillin, the macrolides antibiotics is preferably erythrocin or tylosin. In the invention, an in vitro BF model of streptococcus suis is established, the experiments indicate that the combined use of the beta-monobactams antibiotics and macrolides antibiotics plays a good coordinated synergy role and can eliminate the intramembranous streptococcus suis; the invention further discovers that, when compatibility is carried out between the tylosin and the amoxicillin, the best coordinated synergy role in killing streptococcus suis inside biological capsula is achieved. (coordination synergy is as high as 77.22%).
CN103393616A Tamoxifen citrate tablets The invention relates to tamoxifen citrate tablets which are prepared by the following steps: firstly, preparing tamoxifen citrate to inclusion compounds; and then, preparing the tablets.
EP2226070A1 Process for determining the optimal dosage of antivitamins K in anticoagulant therapy Determining optimal dosage (D o) of vitamin K, comprises: recording value I oof optimal target INR; recording international normalized ratio (INR) values measured in a time T 1; from a gradient P 1, extrapolating and recording a I m a xvalue of INR theoretically reached from the day; recording INR values measured in a period T 2; from the gradient P2, extrapolating and recording a INR I m i n ivalue theoretically reached from the day; calculating difference between INR I m a x iand I m i n ivalues and a factor F; and determining the difference between values I oand I m i n i. Determining optimal dosage (D o) of vitamin K for anticoagulant therapy for achieving and constantly maintaining the value of international normalized ratio (INR) target I opreviously determined by the prescriber according to the pathology of the treated patient, comprises: (a) recording the I ovalue of the optimal target INR; (b) recording the INR values measured in a given time (T 1) by an over dose (D maxi) of the antivitamin K previously determined by the prescriber over the recommended dosage, for determining a first gradient (P 1) of INR values according to the time T 1; (c) from the gradient P 1, extrapolating and recording a I maxvalue of INR theoretically reached from the day where the value I oof the target INR is reached and at the end of a determined period T o; recording the INR values measured in a given period T 2from an underdosing D miniof the antivitamin K fixed by the prescriber below the recommended dosage, for determining a second gradient P 2of values INR according to the time T 2; (d) from the gradient P2, extrapolating and recording a INR I minivalue theoretically reached from the day where the value I oof the target INR is reached and at the end of the fixed period T 0; (e) calculating the difference between the theoretically calculated INR I maxiand I minivalues, a factor F for correcting dose of the antivitamin K expressed by a formula as given in the specification; (g) determining the difference between the values I oof the optimal target INR and I miniof the calculated INR minimum, and the F factor for correcting the antivitamin K dose, the suitable dose D ofor achieving and maintaining a constant value I oof previously fixed INR target using a formula as given in the specification.
CN101138552A Preparation method of almecillin V potassium granular formulation The present invention discloses the preparation method for the penicillin V particles. In the present invention, the problem of low stability of the product is resolved by the technique of dry granulating method. The particles prepared by the invention can be preserved for over 2 years. Because the dry granulating method is applied in the invention, which preserves the activity of the penicillin V, therefore the efficacy is more stable and the safety is more reliable. The present invention is available for technical production.
US7074392 for high penetration into fingernails and toenails; contains humectant for trapping water and liquid nail lacquer containing film forming agent A topical sustained release delivery system for delivery of antifungal agents to the finger or toenails achieving high penetration through the nails by combining the antifingal agent with a keratolytic agent and a humectant. The pharmaceutical sustained release topical preparation is provided in a varnish or spray form for treating the nail and surrounding tissues, where the active ingredient is an antifungal agent, a keratolytic agent, or preferably a combination of an antifuingal and a keratolytic agent. The composition may further comprise an antibacterial, an antiviral, an antipsoriatic agents, or combinations thereof.
WO2008093709A1 Composition for prevention or treatment of disease associated with amyloidosis through inhibition of aggregation amyloid protein and through promotion of degradation of amyloid protein Disclosed are: a means for promoting the degradation of an amyloid protein; and a means for inhibiting the aggregation of an amyloid protein. Specifically disclosed are: a composition for promoting the degradation of an amyloid protein; a composition for inhibiting the aggregation of an amyloid protein; and a composition for preventing or treating a disease associated with amyloidosis, each of which comprises plasmalogen as an active ingredient.
EP1372681B1 Biologically active chloroform fraction of an extract obtained from a mangrove plant salvadora persica l The invention discloses a process of extracting, fractionating and purifying bioactive molecules from an associated mangrove plant, methods of screening for pharmacological activities of crude extract, its fractions and purified compounds and use of the chloroform fraction of the crude extract as anti-spasmodic, anti-arrhythmic and anti-cholinergic agent.
US6936592 antibiotics and antiprotozoa agents The invention relates to a method of preparing compounds of the formula and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.
CN101596201A Application of ergot sterone in preparation of diuresis medicine The invention relates to an application of ergot sterone in preparation of diuresis medicine. Polyporus umbellatus crude drug is mainly used for clearing damp and promoting diuresis and treating dysuria, edema, diarrhea, strangury with turbid urine and morbid leucorrhea. The inventor utilizes diuresis as pharmacological index and screens target area and active ingredients identical with the function of the polyporus umbellatus on the basis of chemical ingredient research on the polyporus umbellatus. Normal saline loaded water retention animal model is adopted for diuresis screening on sterides compound therein, and the ergot sterone is found to have better diuresis effect and is determined as the target area of diuresis of the polyporus umbellatus.
WO2006128674A2 Combinations of indacaterol derivatives and other agents for the treatment of airway diseases A medicament comprising, separately or together, (A) a compound of formula (I) in free or salt or solvate form, where W, Rx, Ry, R1, R2, R3, R4, R5, R6 and R7 have the meanings as indicated in the specification, and (B) one or more of compounds selected from the group consisting of A2A agonists, A2B antagonists, antihistamines, caspase inhibitors, ENaC inhibitors, LTB4 antagonists, LTD4 antagonists and serine protease inhibitors, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.
US7417039 Use of substituted azetidinone compounds for the treatment of sitosterolemia The present invention is directed to the use of sterol absorption inhibiting compounds, pharmaceutical compositions thereof, therapeutic combinations and their use in combination with other lipid lowering agents to treat or prevent sitosterolemia and/or to lower the concentration of sterol(s) other than cholesterol in plasma or tissue of a mammal. Methods of treating or preventing vascular disease and coronary events also are provided.
US20090082410 Constitutively translocating cell line The present invention relates to agonist-independent methods of screening for compounds that alter GPCR desensitization. Included in the present invention are cell lines containing GRKs, in which GPCRs are desensitized in the absence of agonist; the GRKs may be modified. The present invention relates to methods to determine if a GPCR is expressed at the plasma membrane, and if the GPCR has an affinity for arrestin. Modified GPCRs which have increased arrestin affinity are included in the present invention. These modified GPCRs are useful in methods to screen for compounds that alter desensitization, including both the agonist-independent methods and agonist-dependent methods described herein.
EP2468718A1 Cabanillasin, a new antifungal compound, produced by entomopathogenic xenorhabdus cabanillasii Xenorhabdus cabanillasii strain deposited at CNCM having the accession number CNCM I-4418. Antifungal compound purified from Xenorhabdus cabanillasii strain CNCM I-4418 and methods for producing said compound and pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier for use in the treatment of fungal disease.
CN101450938B 7-(4-oximido-3-amido-3-alkyl-1-piperidine)quinoline carboxylic acid derivates and preparation method thereof The invention provides 7-(4-oximido-3-amino-3-alkyl-1-piperidyl) quinoline carboxylic acid derivatives with excellent antibacterial activities and preparation methods thereof and relates to antibacterial agents and feed additives containing the derivatives, in particular to the 7-(4-oximido-3-amino-3-alkyl-1-piperidyl) quinoline carboxylic acid derivatives of the formula (I) which has a substituent of (4-oximido-3-amino-3-alkyl-1-piperidyl) at a 7-position of a carbostyril nucleus. Compared with the prior fluoroquinolone antibacterial drugs, the antibacterial agents have more excellent anti-gram-positive-bacteria activities and broad-spectrum antibacterial activities.
EP1052963B1 Use of alkanoic acid containing compositions for treating nail fungal conditions Compositions and methods for treating keratin-related conditions and disorders such as straightening and styling hair, treating nail fungal conditions such as onychomycosis, ingrown nails, and hyperkeratotic conditions of the epidermis such as psoriasis, acne, callouses, corns, verruca, particularly plantar warts, and surface lines and blemishes of aging skin by aiding the exfoliation of keratinocytes. The compositions comprise at least one alkanoic acid in aqueous solution. The compositions may also be used as shaving creams, additives thereto, and depilatories.
CA2840932A1 Cough reducing product The present invention relates to a product comprising capsaicin or a capsaicinoid for use in the treatment of cough, in particular chronic persistent unexplained cough or increased cough reflex sensitivity. More precisely, the present invention concerns oral formulations for reducing and relieving coughing from other irritants than capsaicin itself. The capsaicin formulations are stated to down-regulate coughing following a regular consumption. Said products can also be used in the treatment of rhinitis and other conditions known to have cough symptoms.
US20080193512 Drug Carrier and Drug Carrier Kit for Inhibiting Fibrosis An astrocyte-specific drug carrier containing a retinoid derivative and/or a vitamin A analog as a constituent; a drug delivery method with the use of the same; a drug containing the same; and a therapeutic method with the use of the drug. By binding a drug carrier to a retinoid derivative such as vitamin A or a vitamin A analog or encapsulating the same in the drug carrier, a drug for therapeutic use can be delivered specifically to astrocytes. As a result, an astrocyte-related disease can be efficiently and effectively inhibited or prevented while minimizing side effects. As the drug inhibiting the activity or growth of astrocytes, for example, a siRNA against HSP47 which is a collagen-specific molecule chaperone may be encapsulated in the drug carrier. Thus, the secretion of type I to type IV collagens can be inhibited at the same time and, in its turn, fibrosis can be effectively inhibited.
US6964979 Liver disorders The invention is directed to a compound and a pharmaceutical composition of the formula: Wherein substitutions at R1, R2 , R3-R12, and Y are set forth in the specification.
US20110230554 Method of Treating Viral Infections by Administration of Ethyl Mercury or Thiol Derivative Thereof Disclosed herein are methods of treating viral infections by administration of ethyl mercury or thiol derivative thereof in an amount effective to treat the viral infection.
CN101016329A Method of preparing cyclopamine from jervine The invention discloses a making method of cyclopamine and application in the medical domain, which comprises the following steps: adopting jervine from Veratrum plant as raw material; reacting jervine and hydrazine hydrate to produce hydrazone in the high-boiling point solvent; denitrifying acted by potassium hydroxide and tert-butanol potassium to form jervine; using carbowax 400 and TEBA as phase transmitting catalyst; connecting tumour cell Hh and Smo protein; dying cancer cell due to non-gene toxicity without influencing normal cell.
US20120282346 Brimonidine compositions for treating erythema The present invention is directed to a pharmaceutical composition including brimonidine tartrate in an amount from about 0.17 percent by weight to about 0.19 percent by weight in a pharmaceutically acceptable carrier such as a gel or cream. The invention also relates to a method of treating erythema in a patient with rosacea by administering the composition of the invention to the site of erythema on the skin of the patient.
US20060166999 Use of microsomal triglyceride transfer protein (MTP) inhibitors for reducing the number of postprandial triglyceride-rich lipoprotein particles (PPTRL) The invention relates to the use of inhibitors of the microsomal triglyceride transfer protein (MTP) for reducing the number of postprandial triglyceride-rich lipoprotein particles (ppTRL) or for reducing their decomposition products i.e. the cholesterol-rich ‘small remnant particle’ (remnants). Said particles are associated with apolipoprotein B-48 (ApoB-48) and are designated as ‘ppTRL’ in the further course of events.
US20090005373 Substituted sulfonamido-macrocycles as tie2 inhibitors and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same The invention relates to substituted sulfonamido-macrocycles according to the general formula (I): in which R1, R2, R4, R5, A, B, C, L, X, Y, Z, n, and m are as defined in the claims, and salts, N-oxides, or solvates thereof, to pharmaceutical compositions comprising said substituted sulfonamido-macrocycles, to methods of preparing said substituted sulfonamido-macrocycles as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
CN101045140A Oral liquor with functions of lower blood sugar, lowering blood pressure and relaxing the bowels An oral liquid for decreasing blood sugar and blood pressure, and preventing and treating hyperglycemia, hypertension, and constipation is proportionally prepared from millet vinegar, VC, oligose, honey and polypeptide.
WO2012013020A1 Anti-fatigue composition, formulation and use thereof An anti-fatigue composition consisting of 20(S)-protopanoxadiol and lycium barbarum polysaccharide. Experiments prove that the composition exhibits a significant anti-fatigue effect. In comparison with the effect attained by the single use of lycium barbarum polysaccharide or 20(S)-protopanoxadiol, the combined use of 20(S)-protopanoxadiol and lycium barbarum polysaccharide exerts an obvious synergistic effect.
CN102697815A Gastrointestinal health-care product The invention relates to the technical field of health-care medicaments and food, in particular to a gastrointestinal health-care product. The gastrointestinal health-care product comprises various strains and dietary fibers in certain ratio. By administration of patients, the health-care product does not have an irritation effect on intestines and stomach, and can be quickly absorbed by gastrointestinal tracts; various probiotics can improve the intestinal immunity, keep balance of intestinal floras, eliminate the intestinal allergy state and fulfill the aims of preventing gastrointestinal diseases; and experiments prove that the health-care product has a remarkable effect, is safe, does not have any toxic or side effect, and can effectively relieve and treat the gastrointestinal diseases by long-term administration.
WO2011144327A1 Posology and administration of glucocorticoid based compositions The present invention relates to an improved method of administration of glucocorticoid based compositions in glucocorticoid replacement therapies enabling an objectively based regimen for administration enabling correct individual dosing of glucocorticoids resulting in an optimised individual replacement therapy and thus an improved long-term outcome for patients with temporary or chronic adrenal insufficiency.
US20120142722 Conjugates of cytotoxic drugs Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders. In another aspect of the invention there is provided a conjugate, comprising a cytotoxic agent and a modulating moiety, the modulating moiety serving to target apoptotic cells.
CN103315991A Application of Nardoaristolones A in preparation of medicine resistant to tubercle bacillus The invention discloses an application of Nardoaristolones A in preparation of a medicine resistant to tubercle bacillus. The invention aims at the present situation that tuberculosis incidence is on the increase and finds that Nardoaristolones A has obvious tubercle bacillus inhibition activity and a good application prospect. The invention discloses an application of Nardoaristolones A in preparation of a medicine resistant to tubercle bacillus for the first time. A brand new skeleton type is adopted, and Nardoaristolones A has unexpected activity for inhibiting tubercle bacillus, no probability that any revelation is given by other compounds, outstanding substantial characteristic and obvious progress when being used for preventing and treating tubercle bacillus infection.
CN101791355A Medicine composition used for preventing birth defects, improving memory and regulating immunity The invention relates to a medicine composition used for preventing birth defects, improving memory and regulating immunity, which comprises atractylis ovata, astragalus mongholicus, boxthornfruit, acanthopanax, fructus ligustri lucidi, vitamin A, beta-carotene, vitamin B complex, vitamin C, vitamin D, vitamin E, major elements (calcium, potassium and magnesium) and trace elements (zinc, selenium, iron, chromium, copper, molybdenum and manganese). The invention is mainly applicable to pregestational women, pregnant women and breast-feeding women, and is effective in the aspects of preventing birth defects, improving the memory and regulating the immunity, and in addition, the invention simultaneously has the health care and benefiting effect, and can not generate any side effect even through long-time application.
US20110009405 Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
US20080154199 Treating an allergic emergency by automatically injecting a first dose of epinephrine and, optionally subsequently, manually injecting a second dose from the same device; both doses have a volume of 0.3 mL of 1 mg epinephrine/ mL of solution; antianaphylactic agents; suitable for children (>12yrs); kits A method of administering epinephrine to a patient includes administering a first dose by automatic injection followed by administering a second dose by manual injection. The first and second injections are administered using the same syringe. In some embodiments, the first and second injections provide the same volume of medicine to the patient. In particular embodiments, the first and second injections have volumes of 0.15 or 0.3 ml.
US7235562 5-trifluoromethyl-N2-indolyl- and quinolinyl-substituted-2,4-pyrimidinediamines, e.g., N2-[3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indol-5-yl]-N4-p-tolyl-5-trifluoromethyl-pyrimidine-2,4-diamine and -[4-(3-Methanesulfonyl-benzylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-3,4-dihydro-1H-quinolin-2-one The present invention relates to a compound of the formula 1 wherein R1-R4 and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
WO2007113005A3 2-substituted 3-aminosulfonyl-thiophene derivatives as aurora kinase inhibitors The present invention provides novel compounds that inhibit cell proliferation, in particular by inhibiting Aurora kinase activity and uses of these compounds for treating, ameliorating or preventing diseases, conditions or disorders benefiting from the inhibition of Aurora kinase activity, in particular hyperproliferative diseases.
US20080312145 Agent for Regulating Bone Formation The present invention provides preventive, ameliorating, and/or therapeutic agents for diseases caused by a disturbed balance between bone formation and bone resorption. The decoys of the present invention induce normal bone metabolism by inhibiting the differentiation-inducing factors of cells involved in bone metabolism. For example, bone resorption can be controlled by using a decoy of the present invention to inhibit NF-κB, a transcriptional regulatory factor that regulates osteoclast differentiation. This method uses a mechanism different from those of previous pharmaceutical agents; therefore, one can expect it to be effective for cases in which existing pharmaceutical agents were not effective.
WO2013191396A1 Novel compound having ability to inhibit 11β-hsd1 enzyme or pharmaceutically acceptable salt thereof, method for producing same, and pharmaceutical composition containing same as active ingredient The present invention relates to a novel compound having the ability to inhibit the 11β-HSD1 enzyme or to a pharmaceutically acceptable salt thereof, to a method for producing same, and to a pharmaceutical composition containing same as an active ingredient. The compound according to the present invention selectively inhibits the activity of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), and can thus be effectively used as a therapeutic agent for treating diseases caused by the excessive activity of 11β-HSD1, e.g. non-insulin dependent (type 2) diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and diseases and conditions brought on by the excessive activity of glucocorticoids.
US7504416 4-substituted quinolines as antitumor agents The invention concerns compounds of formula (I), wherein each of R1, R2, R3, R4, R5, R6, R8, R9, R10 m, n, p, X, Y and Z have any meanings defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-proliferative agent in the treatment of solid tumor disease.
US20060094698 Self-administered contraceptive injection of oily solution The subject invention provides a pharmaceutical formulation in the form of an oily solution for injection to a subject comprising a contraceptively and/or therapeutically effective amount of a long-acting progestogen and a contraceptively and/or therapeutically effective amount of a long-acting androgen dissolved in a pharmaceutically acceptable oily medium wherein the injection is administered by the subject itself with a needle-less device, a mini-needle device or a pre-filled subcutaneous syringe.
US20120093894 Stable cyclosporine containing ophthalmic emulsion for treating dry eyes Disclosed herein are stable oil-in-water emulsion ophthalmic topical liquid compositions having an average particle size less than 1 μm including at least one plant-derived oil other than castor oil wherein the oil comprises only aliphatic side chains free of polar pendent groups. The oil-in-water emulsion ophthalmic topical liquid compositions also include a hydrophilic surfactant having an HLB value between approximately 10 and 14, a vegetable oil-derived hydrophobic non-co-block surfactant having unsaturated side chains that contain less than four oxygen atoms having an HLB value between approximately 4 and 6 and is a liquid at room temperature. The oil-in-water emulsion ophthalmic topical liquid compositions disclosed herein can further include an amount of cyclosporine A or polyphenol in an amount effective to relieve dry eye symptoms.
CN101229182B Antibacterium compounds containing clindamycin hydrochloride The invention discloses an antibacterial composition containing clindamycin palmitate hydrochloride; the antibacterial composition containing clindamycin palmitate hydrochloride of the invention comprises the following components by weight portions: the clindamycin palmitate hydrochloride of 1 portion and the manidipine of 2 to 4 portions. As the clindamycin palmitate hydrochloride has good anti-bacteria activity while the Manidipine has no anti-bacteria activity under the present discovery, the invention combines the clindamycin palmitate hydrochloride with the Manidipine in certain proportional range so that the clindamycin palmitate hydrochloride and the Manidipine can have the function of the cooperative interaction. Without changing the original anti-bacteria activity of the clindamycin palmitate hydrochloride, the combined composition also has the anti-bacteria activity to most of gram-negative bacteria which greatly extends the antibacterial range of the clindamycin palmitate hydrochloride with wide application outlook.
US7091219 Administering an effective amount of bis-sulfonamide hydroxyethyl-amino derivative to a HIV patient to prevent the viral replication Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
US20050014845 Oral administration, bioavailability; no central nervous and cardiovascular side effects A method of treating epilepsy, with the exception of epileptic states, in a patient in need thereof, the method comprising administering to the patient ambroxol or a pharmacologically acceptable salt thereof.
CN101297956B Medicine for treating empyrosis and eczema and producing method thereof The invention relates to an active remedy used for treating burn injury and eczema, and a production method thereof. The active remedy is prepared by components with the following parts by weight: 18 portions of medicinal merbromin, 80 portions of boiling water, 800 portions of purified water or filtered water, 5.5 portions of truestar anisetree, 5.5 portions of radix aucklandiae, 5.5 portions offructus amomi, 5.5 portions of pepper, 5.5 portions of rhizoma zingiberis, 5.5 portions of cinnamon, 5.5 portions of liquorice and 5.5 portions of borneol. The production method is that the medicinalmerbromin is put into a sterilized glass bottle and added with the boiling water to be dissolved, then the purified water or the filtered water, the truestar anisetree, the radix aucklandiae, the fructus amomi, the pepper, the rhizoma zingiberis, the cinnamon, the liquorice and the borneol are added in sequence and then all the dugs and the water are fully stirred and evenly mixed according to the portions, and dipped for 2 to 3 months. After drug juice is fully dissolved out, all dregs of a decoction are removed by a vacuum filter to obtain red liquid medicine. The red liquid medicine is bottled with the cover sealed, thereby the active remedy used for treating burn injury and eczema is prepared. The active remedy of the invention has special formula and preparation method, with obvious treatment effect.
CN101830828A Salen Zn (II) coordination compound and preparation method and application thereof The invention discloses a Salen Zn (II) coordination compound and a preparation method and application thereof. The Salen Zn (II) coordination compound has a cation structure as shown in a general formula (I). The invention optimizes a preparation process of a Salen metal coordination compound, shortens the reaction time and enhances the productivity; and the obtained Salen Zn (II) coordination compound has very good water solubility. The Salen Zn (II) coordination compound forms a coordination bond by utilizing the axial coordination capability of the Salen metal coordination compound and an electron donor contained in a single chain part basic group of an RNA (Ribonucleic Acid) structure and is an RNA composite reagent which has more affinity compared with electrostatic interaction and weak interaction, i.e. hydrophobic interaction, hydrogen bond, Pi-Pistacking, and the like, thereby more effectively blocking the reverse transcription of a reverse transcriptase on virus RNA and providing a certain theoretical foundation for the development of drugs for treating major diseases (such as Aids, cancers, leukemia, and the like) caused by reverse transcriptase viruses.
US20080064728 Heterocyclic Compounds Useful as Dpp-Iv Inhibitors The invention relates to compounds of formula Z-C(R1R2)—C(R3NH2)—C(R4R5)-A (I) wherein Z, R —R and A have the meaning as cited in the description and the claims as examplified by the compound (II) said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.
US20100009998 Compositions and Methods Employing Aminopterin The present invention relates to pharmaceutical compositions containing the antifolate aminopterin, processes for making the compositions, and methods of using them to treat disorders in adult and pediatric patients. Pharmaceutical compositions substantially free of impurities are provided comprising a therapeutically effective amount of aminopterin, or a pharmaceutically acceptable salt thereof. Relative to the teachings of the prior art, the disclosed methods and compositions provide unexpected improvements that include a greater interpatient oral bioavailability in pediatric patients, a smaller interpatient coefficient of variation of oral bioavailability, a smaller mean intrapatient coefficient of variation of oral bioavailability, a greater therapeutic index, a smaller coefficient of variation of toxicity, efficacy in combination therapy, and efficacy of certain polyglutamated metabolites.
WO2013137832A1 Myostatin inhibitors The invention relates to myostatin inhibitors, and in particular, to myostatin inhibitors comprising small molecules, and pharmaceutical compositions comprising the myostatin inhibitors. The invention also relates to methods for treating or preventing a myostatin-related disease or disorder, or methods for increasing muscle growth or muscle regeneration in a subject, or methods for antagonizing myostatin activity in a cell. The invention further relates to methods of identifying compounds that can bind to myostatin.
CN103202844A Compound vitamin (3) pharmaceutical composition for injection and preparation method thereof The invention provides a compound vitamin (3) pharmaceutical composition for injection and a preparation method thereof. The composition is powder injection and comprises vitamin B1, riboflavin sodium phosphate (namely vitamin B2 sodium phosphate), vitamin C, stabilizer glycine and antioxidant thiourea. The preparation method comprises the following steps: preparing liquid medicine, performing activated carbon adsorption, decarburizing, filtering and degerming, filling and performing freeze-drying. The compound vitamin (3) pharmaceutical composition for injection does not contain a pH regulator and is high in stability and high in safety.
CA2388050C Antibiotic caprazamycins and process for producing the same There have been obtained, by cultivation of Streptomyces sp. MK730-62F2 (deposit number of FERM BP--7218), antibiotic caprazamycins A to F having by the following general formula (I) (see formula I) wherein R is tridecyl group, 11-methyl-dodecyl group, and others. These caprazamycins have excellent antibacterial activities against various acid-fast bacteria and various bacteria as well as their drug-resistant strains.
CN101773520A Compound antimicrobial containing polyvalent silver ions and preparation method thereof The invention discloses a compound antimicrobial containing polyvalent silver ions, comprising a compound antibacterial gel preparation, a compound antibacterial water preparation and a compound antibacterial emulsifying preparation which are formed by respectively compounding an antibacterial reagent, a gel reagent, a water reagent and an emulsifying reagent. The antibacterial reagent contains a monovalent silver ion compound, a water soluble chitosan, EDTA, 1-methylbenzotriazole, propylene glycol and one or two of bivalent silver ion compound and trivalent silver ion compound. The invention has strong and lasting bacterial killing capability, can perform quick bacteria killing and deep bacteria killing, has strong anti-inflammatory function and the function on promoting the regeneration of epithelia, and can not generate acute or chronic accumulated toxic or side effect.
WO2012010663A1 2,3,5-trisubstituted thiophene compounds and uses thereof The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
CN101433522A Method for preparing andrographolide solid dispersion The invention discloses a method for preparing a solid dispersion of andrographolidume. The method comprises the following steps: (1) mixing the andrographolidume, kollidon k30 and tween 80 according to the weight ratio of 1 to 5-9 to 0.5-1.5 to obtain a mixture 1, and adding the mixture to absolute ethanol to completely dissolve the mixture 1 to obtain a mixture 2; and (2) heating and vacuumizing the mixture 2 obtained from the step (1) in a water bath at a temperature of between 40 and 70 DEG C to obtain a sticky substance, drying the sticky substance until constant weight, and crushing the dried substance to obtain solid dispersion powder of the andrographolidume. The preparation process at low temperature reduces loss of pharmacological activity of the andrographolidume, and improves the dispersion degree of the andrographolidume in a solid dispersion carrier, thereby further improving dissolution of a medicine; and the prepared solid dispersion has high hardness and good thermal stability, and can be further conveniently prepared into dispersing tablets, capsules and other formulations.
US20130109716 N-aminotetrahydroisoquinolines as anti-cancer agents The compounds herein disclosed are tetrahydroisoquinoline analogs that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of tetrahydroisoquinoline have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC50 values against the breast cancer cells that are 6-10-fold less than the IC50 of tamoxifen.
EP1828156A2 N-biaryl and n-arylheteroaryl piperazine derivatives as modulators of the 5ht2c receptor useful for the treatment of disorders related thereto The present invention relates to certain biarylz and arylheteroaryl piperazine derivatives of Formula (Ia) that are modulators of the 5HT2c receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.
CN103565784A Weight-reducing preparation The invention provides a weight-reducing preparation, relates to novel application of clenbuterol hydrochloride series medicines in the field of pharmacy, and aims to solve the technical problem of weight reducing of an obese patient by means of clenbuterol hydrochloride series medicines. The weight-reducing preparation is characteristics that the weight-reducing function of clenbuterol hydrochloride is sufficiently utilized. The weight-reducing preparation is mainly used for inhibiting, reducing adipopexis, reducing weight, treating obese diseases, and preventing diabetes mellitus, heart disease, cardiovascular and cerebrovascular and other severe internal medicine diseases caused by adipopexis and obesity.
CN102526207A Prescription for treating fish hemorrhagic disease The invention discloses a prescription for treating grass carp hemorrhagic disease. The prescription comprises components including honeysuckle, Picrasma, Radix Isatidis, Forsythia, lignin, photosynthetic bacteria and water. The prescription for treating grass carp hemorrhagic disease has the advantages of remarkable effects, long storage period, long acting period, low cost, and safety to aquatic animals and the environment.
WO2007125287A1 Mono and combination therapy with m1/m4 muscarinic agonist (sabcomeline) for treatment of prodromal syndrome The invention relates to the use of a functional muscarinic M1/M4 agonist or a pharmaceutically acceptable salt thereof to treat prodromal syndrome and in the manufacture of a medicament for the treatment of prodromal syndrome, and to a method of treatment of prodromal syndrome using a functional muscarinic M1/M4 agonist or a pharmaceutically acceptable salt thereof. It also relates to the use of a pharmaceutical composition comprising a functional muscarinic M1/M4 agonist or a pharmaceutically acceptable salt thereof, and at least one cholinergic agent and/or at least one non-cholinergic agent for the treatment of prodromal syndrome, and to a method of treatment of prodromal syndrome by administration of a such a pharmaceutical composition.
US20130035357 Compositions and Methods for Preventing Joint Destruction in Osteoarthritis The present invention is methods for inhibiting collagen destruction in joints of osteoarthritis patients. The methods are based on use of rexinoid compounds, in particular bexarotene, and their activity to inhibit synthesis of matrix metalloproteinases (MMPs) in affected tissue.
EP1546087A1 3-amino-2-hrydroxyalkanoic acids and their prodrugs Compounds having the formula are useful for treating conditions which arise from or are exacerbated by angiogenesis. Also disclosed are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
WO2008114679A1 Bone metabolism ameliorating agent Disclosed is a bone metabolism-ameliorating agent which can ameliorate the bone metabolism in vivo in a chronic renal failure patient who has been received a blood purification therapy such as hemodialysis, hemofiltration or hemodiafiltration. The bone metabolism-ameliorating agent does not contain acetic acid and/or a salt thereof and contains citric acid and/or a salt thereof as an electrolyte, and further comprises other electrolyte and glucose singly or in combination of two or more of them. The bone metabolism-ameliorating agent can take the form of a dialysis solution or a replenisher in dialysis to ameliorate bone metabolism associated with low turnover bone disease, particularly adynamic bone disease or the like.
CN103622979A Preparation method of iron sucrose bulk drug and injection The invention relates to a preparation method of an iron sucrose bulk drug and an injection. The preparation method is characterized in that a ferrous salt and cane sugar undergo a complexation reaction to produce iron sucrose; in the reaction, a stabilizing agent is used so that ferrous ions are not invariably oxidized and enter into a human body. The preparation method creatively improves the existing iron sucrose synthesis method. The iron sucrose prepared from a ferrous salt as a raw material can greatly improve iron sucrose absorption effects, reduce the damage produced by the drug on human body cells, effectively reduce a culture cost and improve iron supplementation effects.
CN103301106A Application for Nardoaristolones A in preparation for anti-hypoxic medicines The invention discloses an application for Nardoaristolones A in preparation of anti-hypoxic medicines. According to the application disclosed by the invention, the anti-hypoxic effect of Nardoaristolones A is observed via an overall and cellular level hypoxic model, and the result indicates that Nardoaristolones A is capable of remarkably increasing the survival rate and survival time of asphyxiant hypoxic mice and acute decompression hypoxic mice, alleviating the myocardial injury of medicine-specificity hypoxic mice, and remarkably protecting the hypoxic injury of in-vitro cultured neonatal rat cardiac myocytes and neurocytes. An application for Nardoaristolones A in preparation of anti-hypoxic medicines is provided.
US20100184824 RNA Interference Mediated Inhibition of Interleukin and Interleukin Receptor Gene Expression Using Short Interfering Nucleic Acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating interleukin and/or interleukin receptor gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of interleukin and/or interleukin receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of interleukin and/or interleukin receptor genes.
US20110237495 Functional metabolomics coupled microfluidic chemotaxis device and identification of novel cell mediators The invention relates to the use of microfluidic chemotaxis device to identify novel active compounds of the metabolome and methods to characterize their actions on cell motility. The invention also includes the active compounds of the metabolome identified by the methods and devices disclosed herein. The results from these in vitro experiments were then correlated with in vivo physiologic responses to identify the downstream effects and therapeutic value. Thus, the invention provides novel methods for treating or preventing second organ injury resulting from ischemia-reperfusion in a patient in need thereof The invention also provides methods of treating, preventing or ameliorating connective tissue degeneration in a patient in need thereof. The invention also provides methods of treating or preventing bone loss. In addition, the invention provides method for inducing bone regeneration in patients in need thereof or preventing bone loss in patients suspected to be in need thereof.
US20110130457 Wax-Based Emulsion for the Treatment of Dry Eye Conditions Disclosed herein is a wax-based emulsion for the treatment of dry eye conditions by reducing the evaporation rate of saline and increasing the viscosity of the tear film. The composition of the present invention comprises an emulsion of wax dispersed in saline. One embodiment of the wax-based emulsion of the present invention comprises a wax in an amount ranging from about 0.001% to about 80% by weight and the remainder saline. In another embodiment, the wax-based emulsion further comprises a hydrocarbon in an amount ranging from about 0.01% to about 80% by weight. In still another embodiment, the wax-based emulsion of the present invention further comprises a cholesterol ester ranging in an amount from about 0.01% to about 80% by weight. In an alternative embodiment, the wax-based emulsion of the present invention further comprises an opthalmic drug in an amount ranging from about 0.01% to about 80% by weight. In yet another embodiment, the wax based emulsion comprises a wax in an amount ranging from about 40% to about 60% by weight, a cholesterol ester in an amount ranging from about 10% to about 20% by weight and the remainder saline. The wax based emulsion may further comprise a hydrocarbon in an amount of up to about 20% by weight. In yet another embodiment, the emulsion further comprises an amount ranging between about 1% to about 20% by weight of standard opthalmic drugs such as antibiotics for delivery to the eye. In some embodiments, the wax of the emulsion is a synthetic wax.
US20110166074 Cln2 treatment of alzheimer's disease A method of treating Alzheimer's Disease may include administering to a subject in need of such treatment a CLN2 therapeutic having beta-amyloid degradation activity.
CN102603613A 4-(methoxycarbonyl)-4-(N- phenylpropionamido)- piperidine-1-substituted compound, preparation method and pharmaceutical application The invention relates to a 4-(methoxycarbonyl)-4-(N- phenylpropionamido)- piperidine-1-substituted compound, a preparation method and pharmaceutical application. The compound is of a structure of free base in a formula (I) or corresponding hydrochloride (I'), wherein in the formula, n is an integral number in the range of 0 to 3 and R is a sulfonyl group or a substituent group with a propofol parent nucleus structure. The compound has excellent water-solubility and stability and can simultaneously have effects of alleviating pain and calming, is suitable for carrying out pain alleviation and calming on a postoperative monitored patient and is particularly beneficial for implementing the operation of the patient on a self-control drug delivery system and the operation of an anesthetist can be reduced. The basic method for preparing the compound comprises the following step that according to the property of the substituent group R, the 4-(methoxycarbonyl)-4-(N- phenylpropionamido)- piperidine-1-substituted compound can be formed by carrying out condensation on a compound with a remifentanil parent nucleus structure and a compound with a corresponding substituent group parent nucleus structure. The invention provides the 4-(methoxycarbonyl)-4-(N- phenylpropionamido)- piperidine-1-substituted compound.
WO2012150890A1 Antibacterial composition A lipid layer forming antibacterial composition that comprises volatile silicon oil, oily lipid, a silver source, and optionally C2-C4 aliphatic alcohol, The silver source is selected from the group consisting of silver salt (Ag+X-), colloidal silver, silver complex, silver particles, silver nanoparticles, and their mixtures. Also disclosed is a method of forming the lipid layer on the skin or a wound, and a method of manufacturing the composition. Preferred ingredients include siloxanes, in particular decamethylcyclopentasiloxane and dodecamethylchclohexasiloxane, with a defined boiling point, and a polar oily lipid, e.g. a membrane lipid such as a phospholipid, glycolipid or sphingolipid.
US20110269720 Minocycline and rifampin microparticles Methods and kits for treating infection associated with implantation of a medical device use of minocycline and rifampin microparticles. The microparticles, in a suitable medium, can be injected in a patient in proximity to the device. The drugs may be configured to be released from the polymer matrix in a controlled manner by manipulation of the properties of the polymer forming the microparticle. By injecting the drugs in the form of microparticles, the drugs can be distributed in a manner so that the entire pocket is protected without affecting device function. The microparticles can be produced aseptically without affecting the manufacturing of the device.
WO2012113503A1 Composition to increase joint and/or postural stability The invention is directed to a composition for the use to increase joint stability or postural stability, wherein said composition comprises branched chain amino acids. It is further directed to the use of branched chain amino acids for the preparation of a food supplement or medicament for the prophylaxis and/or treatment of joint and/or postural instability.
EP1077716B1 Preparation of a medicament for the treatment of gastroesophageal reflux disease A method for the treatment of gastroesophageal reflux disease comprising a combination of active immunization with an anti-gastrin immunogenic composition with an antagonist which blocks or inhibits the gastric acid pump activity; or alternatively administering purified anti-gastrin antibodies with a H2 antagonist or proton pump inhibitor of the gastric acid producing enzyme system.
WO2011159871A3 Compositions and methods for the treatment of addiction, psychiatric disorders, and neurodegenerative disease The present invention features, inter alia, pharmaceutically acceptable compositions that include metyrapol as the sole pharmaceutically active agent; compositions that include metyrapol and at least one additional pharmaceutically active agent; compositions in which the agent targeting the HPA axis is, itself, new or modified (e.g., a bi-specific antibody designed to traverse the blood-brain barrier or a known compound redesigned by, for example, conjugation to a substance that traverses the blood-brain barrier); and compositions in which the agent targeting the HPA axis is newly formulated in such a way that it fails to significantly inhibit cortisol production in the adrenal gland. For example, the composition can be formulated to include a dosage that is too low to reduce plasma cortisol levels or formulated to preferentially affect the skin.
US20120277280 Phenoxy-pyrrolidine derivative and its use and compositions The present invention is directed to the compound 2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.
EP2668941A1 Novel dosage form and formulation of abediterol The present invention provides a pharmaceutical composition in the form of a dry powder for inhalation comprising abediterol or a pharmaceutically acceptable salt in admixture with a pharmaceutically acceptable carrier, providing upon inhalation a dose equivalent to a metered nominal dose of about 1.25 or about 2.5 micrograms of free base abediterol administered with the Genuair® inhaler. The present invention also provides said pharmaceutical composition for use in the treatment of respiratory disease such as asthma and chronic obstructive pulmonary disease COPD.
US20100278914 Fraction of melissa leaf extract having angiogenesis and mmp inhibitory activities, and composition comprising the same The present application describes an ethyl acetate fraction of Melissa leaf having excellent angiogenesis and MMP inhibitory activities, and a composition comprising the same.
CN1683367A Process for preparing lansoprazole sodium salt The present invention relates to the preparation process of lansoprazole sodium possessing ulcer treating effect and with obviously raised stability, flowability and water solubility, and the application of lansoprazole sodium in preparing medicine composition. Free lansoprazole acid is made to react with alkali compound with metal sodium ion to obtain lansoprazole sodium, which is then separated to obtain high purity and high stability lansoprazole sodium in high yield. The technological process is simple and low in cost, and lansoprazole sodium may be used in injection and has less blood vessel irritation, no allergy, no hemolysis and high safety.
WO2011061252A3 Combination of alpha- 2 adrenergic receptor agonist and non-steroidal anti - inflammatory agent for treating or preventing an inflammatory skin disorder Methods and compositions for improved treatment and prevention of an inflammatory skin disorder or a sign and/or symptom associated with the skin disorder are described. The methods involve topical application to the skin a combination of a therapeutically effective amount of an α2 adrenergic receptor agonist, such as brimonidine, and a therapeutically effective amount of a non-steroidal anti-inflammatory agent, such as diclofenac.
CA2318696C Triazepinones, process for their preparation and their therapeutic application The invention relates to compounds of general formula (I) which find an application in the treatment of diabetes.
WO2011096490A1 Imidazopyridin-2-one derivative Disclosed is a prophylactic and/or therapeutic agent for rejection after transplant surgery and for diseases caused by immune system abnormalities, comprising a compound represented by formula (I) or a pharmacologically acceptable salt thereof. In general formula (I), A represents a 8- to 10-membered partially saturated or aromatic fused bicycylic nitrogen-containing heterocyclic group having 1 to 3 nitrogen atoms; A may have the same or different n R1's as substituents; n represents an integer of 0 to 3; B represents a 3- to 7-membered saturated or partially saturated monocyclic hydrocarbon group and may contain 1 or 2 oxygen atoms, sulfur atoms, nitrogen atoms, sulfinyl groups or sulfonyl groups as ring constituents; B may have the same or different m R2's as substituents; R2 represents a substituent present on a carbon atom or a nitrogen atom which forms B; and Q represents a bond or a C1-4 alkylene group.
US20120107251 Oregano oral care compositions and methods of use thereof A multi-benefit oral composition is provided. The oral composition is efficacious as an antibacterial, antiplaque, anti-inflammatory, anti-oxidant, and anti-halitosis oral composition. The active ingredient has one or more active compounds from an extract of oregano. The oral composition can be in the form of a mouth rinse; a dentifrice, including toothpaste, gels, powders; animal products; a film; or confectionaries, such as lozenges, and the like. Methods of making and using the oral composition are also provided.
WO2012066065A1 Phenyl-heteroaryl amine compounds and their uses The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
US20080114011 Antitumor agents, anticancer agents; synergistic mixture; side effect reduction; inhibiting tumor growth in cancer patient by administering a combination therapy comprising 5-Fluorouracil (5-FU) and a methylol transfer agent capable of enhancing antineoplastic effect of 5-FU Tumor growth and metastases in cancer patients are inhibited by administration of a combination therapy including effective amounts of 5-Fluorouracil and a methylol transfer agent such as taurolidine, taurultam or mixtures thereof.
CN101147742A Medicinal composition containing licorice total flavone and alooerine The present invention relates to a medicinal composition containing licorice total flavone and alooerine. It can be used for curing arrhythmia and viral diseases due to various causes.
US20060046999 Monocyclic aroylpyridinones as antiinflammatory agents The present invention relates to monocyclic aroylpyridinones, processes for their preparation, and their use in medicaments, especially for the treatment of COPD: (formula I).
EP2017251A1 Method for stabilization of reduced coenzyme q10 The present invention aims at providing a method of stabilizing reduced coenzyme Q10 useful as food, food with nutrient function claims, food for specified health use, nutritional product, nutritional supplement, animal drug, drink, feed, cosmetic, pharmaceutical product, therapeutic drug, prophylactic drug and the like, as well as a composition thereof. The present invention provides a method of stabilizing reduced coenzyme Q10, including achieving the co-presence of reduced coenzyme Q10 and reduced coenzyme Q9 and/or reduced coenzyme Q11, and a composition containing reduced coenzyme Q10 and reduced coenzyme Q9 and/or reduced coenzyme Q11.
WO2014090127A1 Cyclodextrin carrier-based arteannuin compound conjugate and preparing method thereof Disclosed are a cyclodextrin carrier-based arteannuin compound conjugate and a preparing method thereof. Molecules of an arteannuin compound are connected by using an ester bond formed between a carboxyl group of the molecules of the arteannuin compound and a hydroxyl group of the cyclodextrin.
CN103239445A Regulating effect of 5-HT2C receptor-specific blocker on basic rhythmical respiration discharge of mammal medulla oblongata The invention discloses a novel use of a 5-HT2C receptor-specific blocker, namely regulating effect of the 5-HT2C receptor-specific blocker on basic rhythmical respiration discharge of mammal medulla oblongata. The invention provides an application of the 5-HT2C receptor-specific blocker in preparing a product, and the functions of the product are as indicated in (a) and/or (b) and/or (c): (a) shortening the inspiratory time of basic rhythmical respiration discharge of a hypoglossal nerve root; (b) prolonging the respiratory cycle of basic rhythmical respiration discharge of the hypoglossal nerve root; and (c) reducing the discharge integral amplitude of basic rhythmical respiration discharge of the hypoglossal nerve root. The invention discovers and functionally proves that adjustment of basic rhythmical respiration discharge participated in by the 5-HT2C receptor exists on a newborn rat in vitro medulla oblongata slice.
EP1806144A2 Use of SARP-1 for the treatment and/or prevention of scleroderma The invention relates to the use of SARP-1 for the preparation of a medicament for the treatment and/or prevention of scleroderma, in particular of systemic sclerosis.
CN1830961A Process for preparing medicine for treating glycuresis, application of its pharmaceutical prepn. A process for preparing the medicine used to treat diabetes B and its capsules or tablets is disclosed. Its advantages are simple route and low cost.
CN102813724A Digestion-promoting and stomach-strengthening decoction The invention discloses a digestion-promoting and stomach-strengthening decoction which is prepared from the raw materials of, by weight: 13-17 parts of pilose asiabell root, 10-14 parts of upright ladybell root, 10-14 parts of hawthorn fruit, 4-8 parts of lemon slices, 1-5 parts of golden thread, 7-11 parts of medicinal evodia immature fruit, 10-14 parts of parched hawthorn fruit, 7-11 parts of vinegar powder, 4-8 parts of panax notoginseng, 28-32 parts of ark shell, 13-17 parts of common bombax root, 1-5 parts of the cajanus cajan, 8-12 parts of medicinal fermented mass, 4-8 parts of ghostplant wormwood herb, and 1-5 parts of Chinese brake herb. According to the invention, the parched hawthorn fruit and the hawthorn fruit have functions of gastric motility increasing, gastric emptying promoting, and fullness symptom ameliorating. Upright ladybell root has functions of stomach-Yin nourishing and digestion difficulty symptom ameliorating. Panax notoginseng has a gastric mucosa repairing function. Golden thread has functions such as killing intragastric helicobacter pylori. Vinegar powder is solid vinegar. Lemon has an appetite promoting function. The whole formula is reasonably and scientifically formulated, and has a good curative effect against digestion difficulty, fullness, and stomachache symptoms caused by acute or chronic gastritis. The decoction has no toxic or side effect.
US20100292170 Methods for diagnosing and treating pelvic pain disorders via beta-catenin Methods for diagnosing a pelvic pain disorder that include analyzing samples for increased levels and/or nuclear accumulation of beta-catenin, which indicates presence of the pelvic pain disorder, particularly interstitial cystitis. Therapeutic treatment of a pelvic pain disorder, particularly interstitial cystitis, includes the administration to a patient of an effective amount of an inhibitor of beta-catenin activity. This can be carried out by direct administration of the therapeutic agent or via gene therapy.
WO2007012379A2 Use of 3-hydroxycoumarin derivatives The invention relates to the use of 3-hydroxylcoumarin derivatives of general formula (I) or the physiologically acceptable salts thereof or a preparation containing at least one compound of formula (I), wherein R1 to R4 can be the same or different and are selected from -H, -OH, -OA, -A, -OCOA, R1 and R2 together can be methylene dioxy or ethylene dioxy, and A represents alkyl or R-substituted alkyl radical, phenyl or R-substituted phenyl radical, for improving the general state of the skin, and for the prophylaxis and/or treatment of skin diseases, especially hyperpigmentation.
US7504410 such as N-[3-[[5-bromo-4-[[3-[[[1-(trifluoromethyl)cyclobutyl]carbonyl]amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide; Chks (checkpoint kinases), Akts (protein kinases B) and Pdks (phosphoinositide-dependent kinases) inhibitors; antiproliferative agents This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseases.
CN103520165A Application of indeno triazine compounds as substrate of quinone oxidoreductase depending on NAD (P) H The invention discloses application of indeno triazine compounds as a substrate of quinone oxidoreductase depending on NAD (P) H. The indeno triazine compounds are catalyzed through the quinone oxidoreductase depending on the NAD (P) H to generate an oxidation reduction cycle reaction, a large number of reactive oxide free radicals are generated, strong oxidative stress is induced, and the obvious lethal effect on lung cancer, liver cancer, cervical cancer, pancreatic cancer, breast cancer, prostate cancer, nasopharynx cancer, kidney clear cell carcinoma, oral epidermoid carcinoma, chronic myelogenous leukemia, intestinal cancer, brain cancer, gastric cancer, esophagus cancer and other cancer cells expressed by the quinone oxidoreductase depending on the NAD (P) H is achieved. The indeno triazine compounds used as the substrate of the quinone oxidoreductase depending on the NAD (P) H can also be used as sensitizers for treating the cancer with radiotherapy, and have the obvious anticancer synergistic effect. In addition, the indeno triazine compounds used as the substrate of the quinone oxidoreductase depending on the NAD (P) H have antibacterial and antifungal activity.
US20090149430 Composition containing amidine derivatives or carboxamide derivatives and steroids, as a medicament The present invention relates to a composition containing at least one amidine derivative or carboxamide derivative of general formula (I) or (A) in combination with at least one compound chosen from steroids, corticoids or corticosteroids, wherein said composition is suitable for the preparation of a medicament.
CN101235069A Oleanane derivative with carbonyl and oxygen substituent at C ring and use thereof The invention provides an oleanane derivative which C ring is provided with carbonyl and oxygen substituent, represented as formula (1). The inventive compound can inhibit the growth activity of tumor cell to be applied in anti-tumor drug and can inhibit mice ear swelling caused by dimethylbenzene to be applied in anti-inflammatory agent. The formula (1) is represented as above.
CN102695509A Novel photosensitizer formulations for oral administration The present invention provides novel drug formulations for oral administration for diverse medical applications including anticancer, antimetastatic, antibacterial, antifungal, antiprotozoic, antiviral, antiprionic and PDT treatments for diagnostic and therapeutic purposes. In a preferred embodiment the oral drug formulation comprises a photosensitizer and suitable excipients and may be administered in multiple doses over an extended period of time with exposure to activating radiation occurring generally between individual doses or in a light-independent manner. In another preferred embodiment PDT methods for treating hyperplasia and neoplasia, for localizing hyperplasic and neoplasic tissues and pathogen bacteria by fluorescence, for treating infections caused by pathogen bacteria in complex body fluids and for fat reduction, skin disorders and vascular diseases are provided.
CN103381156A Applications of Chukrasone B in anti-tubercle bacillus medicines The invention discloses applications of Chukrasone B in preparation of anti-tubercle bacillus medicines. At present, morbidity of tuberculosis is high, mycobacterium trberculosis multiple-resistant strains are found, and morbidity and mortality of tuberculosis are on the rise, so that application prospect of the remarkable inhibitory activity of Chukrasone B on tubercle bacillus is promising. The applications of Chukrasone B in preparation of anti-tubercle bacillus medicines are disclosed for the first time. Due to the fact that skeleton type belongs to completely novel skeleton type, and Chukrasone B has an unexpectedly high inhibitory activity on tubercle bacillus, probability of other compounds giving any revelation for Chukrasone B does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in treating of tubercle bacillus infection.
US20120010255 Compounds and Methods for Regulating Integrins The application describes small molecules capable of modulating activity of beta2 family of integrins, such as integrin CD11b/CD18 (also known as Mac-1, CR3 and αMβ2). Such compounds may be used in certain embodiments for treating a disease or condition, such as inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, wound-healing, organ transplantation and cardiovascular disease, among others.
WO2006106915A1 PROTECTIVE AGENT FOR RETINAL NEURONAL CELL CONTAINING PROSTAGLANDIN F2α DERIVATIVE AS ACTIVE INGREDIENT It is intended to find a novel pharmaceutical application of a prostaglandin F2α derivative. It was found that the prostaglandin F2α derivative inhibits glutamate-induced retinal neuronal cell death in a concentration-dependent manner in the retinal neuronal cell of rat fetus, in other words, the prostaglandin F2α derivative acts directly on the retinal neuronal cell and exerts a protective effect. Accordingly, the prostaglandin F2α derivative is useful in the prevention or treatment of eye diseases related to retinal neuronal cell damage.
WO2005004862A3 Method for photodynamic inactivation of pathogens using ala The invention relates to a method for inactivating pathogens, particularly viruses and bacteria in a biological fluid comprising blood cells. The method comprises the steps: preparation of, or placing of the fluid in a container, at least a part of the walls of which are transparent to radiation with a wavelength between 350 nm and 450 nm, introduction of the 5-aminolevulinic acid (ALA), or a derivative thereof into the fluid, such as to allow the transformation of the ALA into protoporphyrin IX, irradiation of the container with at least one radiation of wavelength between 350 nm and 450 nm such that, on activating the protoporphyrin IX, the pathogens are inactivated, whereby the fluid has the leukocytes removed prior to the introduction of the ALA.
CN102164591A Combinations of a rate control agent and an A-2-alpha receptor antagonist for use in multidetector computed tomography methods This invention relates to methods for multidetector computed tomography myocardial perfusion imaging comprising administering doses of a rate-control agent and one or more adenosine A2A receptor agonists to a mammal.
US20090124644 Hiv inhibiting 2-(4-cyanophenylamino) pyrimidine derivatives HIV replication inhibitors of formula pharmaceutically acceptable addition salts or stereochemically isomeric forms thereof, wherein X is NR4, S, SO or SO2; the preparation of these compounds as well as pharmaceutical compositions comprising these compounds; the use of these compounds for the prevention or the treatment of HIV infection.
CN1965838A Pharmaceutical composition containing cefpiramide and beta-lactamase inhibitor The invention relates to a drug composite with cooperate antibiosis function, and relative production, wherein it comprises cephalosporin or its salt, and beta-lactamase restrainer (clavulanic acid, methmazole, etc) at 10:1-1:10 ration. Said composite has better antibiosis effect on single cephalosporin, etc.
CN1813743A External-use formulation of levocetirizine hydrochloride The present invention relates to a medicine levocetirizine hydrochloride preparation for external application. Said preparation is made up by using levocetirizine hydrochloride as active effective component and medicinal auxiliary material, and can be used for effectively curing various dermal allergic diseases.
US7030100 Analgesic inhibitor of isoforms of cyclic guanosine monophosphate (cGMP)-dependent protein kinase I alpha (PKGI alpha); drug screening Several lines of evidence have shown a role for the nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) signaling pathway in the development of spinal hyperalgesia. However, the roles of effectors for cGMP are not fully understood in the processing of pain in the spinal cord. cGMP-dependent protein kinase (PKG) Iα but not PKGIβ was localized in the neuronal bodies and processes, and was distributed primarily in the superficial laminae of the spinal cord. Intrathecal administration of an inhibitor of PKGIα, Rp-8-[(4-Chlorophenyl)thio]-cGMPS triethylamine, produces significant antinociception. Moreover, PKGIα protein expression was dramatically increased in the lumbar spinal cord after noxious stimulation. This upregulation of PKGIα expression was completely blocked not only by a neuronal NO synthase inhibitor, and a soluble guanylate cyclase inhibitor, but also by an N-methyl-D-aspartate (NMDA) receptor antagonist, MK-801. Noxious stimulation not only initially activates but also later upregulates PKGIα expression in the superficial laminae via an NMDA-NO-cGMP signaling pathway, suggesting that PKGIα plays an important role in the central mechanism of inflammatory hyperalgesia in the spinal cord.
US20100197800 Treatment and/or Prevention of Presbycusis by Modulation of Metabotropic Glutamate Receptor 7 The invention relates to the treatment and/or prevention of age-related hearing loss (presbycusis) with a modulator of a metabotropic glutamate receptor 7 (mGluR7).
WO2014049515A1 Pyrrolidine substituted flavones for treatment of renal cystic diseases The present invention relates to the pyrrolidine substituted flavones, represented by the compounds of formula 1 (as described herein) or stereoisomers, or tautomers thereof, or pharmaceutically acceptable salts or solvates thereof, for use in the treatment of renal cystic diseases. The present invention also relates to pharmaceutical compositions containing said compounds for use in the treatment of renal cystic disease.
CN103405454A Application of Chukrasone A in medicaments for treating renal carcinoma The invention discloses an application of Chukrasone A in preparing medicaments for treating renal carcinoma, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluation finds that the Chukrasone A also has a significant inhibitory effect on the growth of a human renal carcinoma cell strain KC. Therefore, the Chukrasone A can be used for preparing anti-renal carcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating renal carcinoma provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to renal carcinoma cells.
WO2012119458A1 Synthesis and use of antitumor drug lqc-y Disclosed are the general structural formula of LQC-Y as well as the synthesis and use thereof. Pharmacological experiments demonstrated the marked antitumor effect of such compounds. Single day administration of LQC-Y3 to mice at a maximum dose of 6000 mg/kg showed no toxicity response during the 14-day continuous observation period, indicating the high safety of the compounds, and can be used to prepare medicaments for preventing and treating carcinomas such as liver cancer, lung cancer. (General structural formula of LQC-Y) R represents steroid compounds such as cholic acid, deoxycholic acid, ursodeoxycholic acid, chenodeoxycholic acid, and hyodeoxycholic acid; triterpenoid compounds such as oleanolic acid, ursolic acid, pachymic acid, glycyrrhetinic acid and glycosides thereof; emodic acid, emodin and other mono-substituted or poly-substituted structures of anthraquinone core; baicalein, baicalin and other flavone-like compounds; shikimic acid, mono-substituted shikimic acid or poly-substituted shikimic acid; geniposidic acid and other iridoid acid derivatives; paeonol, curcumin and structureal derivatives thereof.
CN101843621B TS-1 granules and preparation method thereof The invention belongs to the technical field of medicaments, and relates to TS-1 granules for treating advanced gastric cancer and a preparation method thereof. The method comprises the following steps of: preparing active medicaments tegafur, gimeracil and potassium oxonate into a cyclodextrin inclusion compound; and sieving the inclusion compound, uniformly mixing the sieved inclusion compound and pharmaceutically acceptable auxiliary materials and performing wet granulation or dry granulation to prepare the granules. The granules have the advantages of increasing the water solubility and stability of the medicaments, covering the bitter taste of the tegafur, prolonging the action time, improving the medication compliance of patients with cancer, greatly improving the bioavailability ofthe medicaments and reducing the toxic or side effect of the medicaments.
CN102526095A Medicinal composition for treating catarrh The invention provides a medicinal composition for treating catarrh. The medicinal composition consists of montmorillonite, xylitol and water. The medicinal composition is fast in effect, good in curative effect, low in taking frequency and free of toxic and side effect.
WO2008080461A1 5-phenyl-6-pyridin-4-yl-1,3-dihydro-2h-imidazo[4,5-b]pyridin-2-one derivatives useful as a2b adenosine receptor antagonists A compound of formula (I) wherein: G1 is selected from the groups consisting of fluorine and chlorine atoms, G2 is selected from the groups consisting of hydrogen, fluorine and chlorine atoms, and G3 is selected from the groups consisting of fluorine and chlorine atoms and pharmaceutically acceptable salts or N-oxides thereof.
CN101848922A Novel mangiferin calcium salts, the method for its preparation and its use The present invention provides a mangiferin calcium and its preparation and use. The mangiferin calcium can lower plasma insulin, glucose, lipid, and also can improve the solubility and oral bioavailability of mangiferin and increase insulin sensitivity.
CN102151242B In-situ gel slow-release preparation for anti-tuberculosis drugs and preparation method thereof The invention discloses an in-situ gel slow-release preparation for local drug delivery, which comprises drug active ingredient microspheres and in-situ gel. The in-situ gel slow-release preparation is characterized in that the gel forming temperature is kept within the scope of 15-25 DEG C and the calcium ion effect exists; the drug active ingredient is anti-tuberculosis drugs; the proportional relationship of the drug active ingredient microsphere and the temperature-ion sensitive gel is 5-50 mg:1-50 ml; the drug active ingredient microspheres are uniformly dispersed in the in-situ gel under the agitation condition; the in-situ gel slow-release preparation can restrain the excessive release of the drugs and lead the drugs to release stably and detain at the lung of a rat for 120 h at most; and a drug system detains at the local part for a long time, thereby realizing the treatment purpose.
WO2007032699A1 (+)-and-(-)-trans-2,3,4,4a,5,9b-hexahydro-2,8-dimethyl-1h-pyrido[4,3-b] indole optical isomers The invention relates to novel optical isomers, which are isolated according to the inventive method, embodied in the form of optical antipodes with respect to each other, exhibit the individual biological power and can be used in the form of an active ingredient in nootropic and sedative pharmaceutical compositions for treating different individual states of patients.
CA2728563A1 Use of mifepristone for the treatment of amyotrophic lateral sclerosis The invention generally pertains to the discovery that agents capable of inhibiting the binding of cortisol to its receptor can be used in methods for treating patients diagnosed with Amyotrophic Lateral Sclerosis (ALS).
WO2014108759A1 INHIBITORS OF miRNAs 221 AND 222 FOR ANTI-TUMOR ACTIVITY IN MULTIPLE MYELOMA The present invention refers to inhibitors of miRNAs 221 and 222, and to their use as medicaments in the treatment of multiple myeloma. The present invention relates also to inhibitors of miRNAs 221 and 222 of the type of LNA- miRNAs and having formula +C*A*G*+A*+C*A*+A*T*+G*T*+A*+G*C, and formula C*+A*+G*+A*T*+G*T*+A*+G*C wherein letters with symbol " + " indicate the positions of LNA and symbol "*" indicates phosphorothioate bonds.
US20090247583 Pharmaceutical composition comprising, in combination, saredutant and paroxetine A subject-matter of the present invention is pharmaceutical compositions comprising, in combination, at least one active ingredient chosen from (S)-(−)-N-[4-(4-acetamido-4-phenylpiperidin-1-yl)-2-(3,4-dichlorophenyl)butyl]-N-methylbenzamide and pharmaceutically acceptable salts thereof and at least one second active ingredient chosen from trans-(−)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine and pharmaceutically acceptable salts thereof.
WO2012106584A3 Pitavastatin salts The present disclosure includes salt of pitavastatin, and processes for their preparation and isolation. It further relates to crystalline forms of pitavastatin salts and hydrates thereof, and process for preparing an amorphous form of pitavastatin
US20080221118 Tetrahydroquinoline Derivatives Compounds of the formula I, in which s, k, I, W, R1, R2, R3, and U have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.
CN103505510A Refreshing agent The invention relates to a spray capable of reviving and refreshing, and especially relates to a refreshing agent made from natural raw materials. The refreshing agent comprises, by weight, 30 to 50% of oxygen and 50 to 70% of a plant extract; the plant extract comprises, by weight, 0.1 to 2% of borneolb, 0.1 to 2% of menthe, 0.1 to 1.5% of eucalyptus oil, 0.01 to 1% of bear gall powder, 0.1 to 0.5% of bepearl powder, 0.1 to 5% of a spice, and the balance water. The refreshing agent is sealed in bottles, and it just need to press a spray head for spraying. According to the refreshing agent, oxygen is used for pressurizing, and is capable of increasing oxygen content of surrounding environment so as to avoid oxygen deficit tiredness caused by closed environment. The refreshing agent is capable of relieving sleepiness, refreshing, resisting fatigue, helping to focus attention, increasing work and study efficiency, reducing mental stress, relieving asthenopia, replenishing skin water, and supplying oxygen needed by human body.
WO2011017600A2 Compositions and methods for treating beta-amyloid related diseases In alternative embodiments the invention provides compositions and methods for ameliorating diseases and conditions having a beta-amyloid component, including Alzheimer's disease (AD), Vascular Dementia (VD), dementia, pre-dementia, Cognitive Dysfunction Syndrome (CDS) and loss of cognition in humans and in non-human animal. In alternative embodiment the invention provides analogs of AB-007 and its acid form E64c (loxistatin), their preparation, and pharmaceutical compositions thereof and methods of making and using same. In alternative embodiments compositions of the invention are deuterated analogs of AB-007 (or E64d) and E64c (or loxistatin). In alternative embodiments compositions of the invention are metabolically blocked forms as compared to AB-007 and loxistatin. In alternative embodiments compositions of the invention are used to ameliorate (including treat, slow, reverse or prevent) a disease or condition which can be ameliorated by partial or complete inhibition of a cysteine protease, e.g., AD, VD, CDS. The invention also provides alternative dosage forms and formulations for AB-007 and loxistatin, and for compounds of this invention, which can be used e.g., to treat AD, VD and CDS, in humans and in non-human animals.
US20110123480 Chimeric proteins and uses thereof The present invention provides a chimeric protein capable of killing or modifying a cell expressing abnormally high levels of a ligand of a receptor of the TNF/NGF family, comprising the amino acid sequence of at least one polypeptide consisting of an extracellular portion of said receptor connected to an effector molecule. In addition the invention provides pharmaceutical compositions comprising said chimeric protein and use thereof.
CN103006645A Application of 2-aminobenzothiazole derivatives being taken as DHODH (dihydroorotate dehydrogenase) inhibitor The invention relates to applications of 2-aminobenzothiazole derivatives in pharmaceutical chemistry and pharmacotherapy. Specifically, the invention relates to applications of a compound shown in formula I (described in the specification) and a medicinal composition of the compound in preparation of medicines used for treating diseases related to DHODH.
US7288534 Sphingomyelin enhancement of tumor therapy Cytotoxic tumor therapy in a patient is enhanced by co-administration of sphingomyelin. The invention most likely enhances a tumor cell's ability to undergo ceramide-induced apoptosis by increasing the levels of sphingomyelin in all cellular compartments, thereby providing sufficient substrate for activated sphingomyelinase. A method of treating rheumatoid arthritis also is provided.
CA2754943A1 Substituted 3-amino-2-mercaptoquinolines as kcnq2/3 modulators The invention relates to substituted 3-amino-2-mercaptoquinolines, methods for the production thereof, medicaments containing said compounds, and the use of said compounds for producing medicaments.
CN102178675A Application of quercetin and composition thereof to preparation of anti-hypoxia medicaments The invention provides application of quercetin to preparation of anti-hypoxia medicaments. The invention also provides a composition. The composition comprises the quercetin with pharmaceutical effective dose, a pharmaceutically acceptable auxiliary material and chlorogenic acid and/or protocatechuic acid with pharmaceutical effective dose. The quercetin and the quercetin-containing composition can be widely applied to developing and preparing more effective and low-toxicity anti-hypoxia natural medicaments due to the activity in the anti-hypoxia aspect, and have a wide application prospect.
WO2013059634A9 Use of cdk9 inhibitors to reduce cartilage degradation The present invention relates to the use of cyclin-dependent kinase 9 (CDK9) inhibitors to reduce, inhibit and/or prevent cartilage degradation. CDK9 inhibitors can be used to reduce, inhibit and/or prevent cartilage degradation and loss of cartilage viability during allograft storage. CDK9 inhibitors can be used as a post-injury intervention treatment to reduce, inhibit and/or prevent the acute cellular responses that lead to future cartilage degradation and osteoarthritis.
US20120329880 Method of preparing oil suspensions of carotenoid with low viscosity and high fluidity and use thereof The present invention relates to a method of preparing for an oil suspension of carotenoid with low viscosity and high fluidity and use thereof. The method comprises the following steps: mixing carotenoid crystals with tetrahydrofuran, heating the mixture to reflux temperature 50˜70°C. under stirring to dissolve the crystal, filtering and condensing to obtain the concentrate; mixing the concentrate with ketone solvent, heating the mixture to reflux temperature 60-80□ to dissolve the concentrate, filtering, condensing, adding absolute alcohol, crystallizing under stirring at room temperature, filtering and drying in vacuum to obtain carotenoid crystals; mixing carotenoids crystals after granded with plant oil or grinding carotenoid crystals with plant oils and then adding plant oil, to obtain the oil suspension of carotenoid with low viscosity and high fluidity. While the content of carotenoid is 10.0˜45.0 wt. % in the oil suspension of carotenoid obtained from the present invention, the oil suspension of carotenoid has high fluidity at temperature 5˜25□, and in the meanwhile do not need any extra heating steps during applications.
WO2007046318A1 Liquid preparation for external application containing indomethacin Disclosed is a liquid preparation for external application which contains indomethacin. This liquid preparation for external application is excellent in feeling of use and absorbability, and does not deposit crystals over time even in a low temperature environment. Specifically disclosed is a liquid preparation for external application containing indomethacin, a lower alcohol, water, a sulfite and a polyethylene glycol having an average molecular weight of 3,000-15,000.
CN1994286A Application of total curcumin in preparation of medicine for preventing and postponing chronic kidney function failure The invention relates to an application of curcumin in drug preparation, wherein test has proves that curcumin can increase the food intake of renal failure mouse, increase weight and improve health, it can improve Hb, RBC, and reduce NO, TNF-a contents, improve SOD level and release the renal failure condition.
US8716269 Combination of pilocarpin and methimazol for treating Charcot-Marietooth disease and related disorders The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related peripheral neuropathies. More particularly, the invention relates to combined therapies for treating said disease by affecting simultaneously muscarinic receptor signaling and thyroid hormone pathway in a subject.
US20050250840 treating, or lessening the severity of, diabetic nephropathy in an adult human patient in need thereof by administering to patient 500 mg mycophenolate mofetil and 5 mg lisinopril The present invention relates to a method of treating diabetic nephropathy with a combination of an immunosuppressive agent and an ACE inhibitor.
US20100204186 Aromatic a-ring derivatives of tetracycline compounds Aromatized A-ring derivatives of tetracycline compounds are described.
WO2010079238A1 Heterotricyclic compounds as positive allosteric modulators of metabotropic glutamate receptors The present invention relates to novel compounds of Formula (I), wherein wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors - subtype 4 ("mGluR4") which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
WO2009113810A3 Pharmaceutical composition, use thereof, and method for the treatment or prevention of allergic and autoimmune diseases The present invention provides a pharmaceutical composition for preventing or treating allergic or autoimmune diseases, which contains immunoglobulin, as an active ingredient, isolated from the blood of a patient who is suffering from an allergic or autoimmune disease. In addition, the disclosed invention provides another pharmaceutical composition for preventing or treating allergic or autoimmune diseases, which contains immunoglobulin isolated from the blood of another patient who is suffering from an allergic or autoimmune disease as an active ingredient. The present invention also provides a manufacturing method and a medicinal and pharmaceutical use of the composition of a medicine for preventing or treating allergic or autoimmune diseases. Also, the disclosed invention provides a method for preventing and treating allergic or autoimmune diseases, which includes administering the pharmaceutical composition to mammals. By administering the disclosed pharmaceutical composition to mammals, allergic or autoimmune diseases, which are hard to control with a current standard drug treatment method, can be treated. Therefore, through the pharmaceutical composition, the use thereof for preventing or treating allergic or autoimmune disease, and the prevention and treatment method using the same, allergic or autoimmune diseases whose symptoms are not easily treated with current standard drug treatment methods can be more effectively treated.
WO2009037467A1 Pyrrolopyrimidine compounds Compounds of formula (I) are A2B receptor antagonists: wherein Ri is optionally substituted aryl or an optionally substituted monocyclic heteroaryl group having 5 or 6 ring atoms; R2 and R3 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-(C1- C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-(C1- C6)-alkyl; R4 and R5 are independently selected from hydrogen, optionally substituted C1-C6 alkyl, optionally substituted aryl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, -NHR7-N(-R8)-R9, -NH-(C=O)-R10, -(C=O)- NH-R11, -(C=O)-O-R12, or halo; R6 is hydrogen, C1-C6 alkyl, aryl-(C1-C6)-alkyl, - (C=O)-NH-R13, -(C=O)-R14, aryl, heteroaryl, hydroxy-(C1-C6)-alkyl, or C3-C8 cycloalkyl-alkyl; and R7, R8, R9, R10, R11, R12, R13 and R14 are independently selected from C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl and heteroaryl.
US20110268800 Unsaturated fatty acids as thrombin inhibitors A preparation having at least one unsaturated fatty acid and the use of at least one unsaturated fatty acid having a chain length of 18 or 20 carbon atoms and of plant drugs containing the unsaturated fatty acid as a free fatty acid or a fatty acid radical of a triglyceride. The fatty acid has a chain length of 18 carbon atoms which are provided with 1 to 3 double bonds and the fatty acid has a chain length of 20 carbon atoms which are provided with 1 to 4 double bonds. The double bond or one of the double bonds are located in position 9 or 11 of the carbon chain. The unsaturated fatty acid is supplied in the all-cis configuration. The at least one unsaturated fatty acid prevents and/or treats or is used for producing a preparation for preventing and/or treating thrombosis and thromboembolic diseases.
EP1845987A2 Treatment of inflammatory disorders with praziquantel The present invention refers to a method of treating inflammatory disorders, in particular autoimmune disorder (e.g. arthritis), which consists in the administration of praziquantel or a pharmaceutically acceptable salt thereof.
US20110105474 Heterocyclic derivatives as hdac inhibitors This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; R1 is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl or C1 C6 haloalkoxy; R2, R3 are, independently, hydrogen; C1-C6 alkyl; aryl; or taken together with the carbon atoms to which they are bound form a bridged bicyclic ring or a fused heterocycle; X is CH or nitrogen; Y is a bond, oxygen, (CH2)mCR4R5(CH2)n, or (CH2)oNR6(CH2)p; m, n, o, p, R4, R5 and R6 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
US20130039960 Compositions for reduction of side effects The present invention provides drug therapy formulations. In some embodiments, the present invention provides combinations of pharmaceutical agents (e.g., stimulant and non-stimulant), pharmaceutical formulations (e.g., nanoparticulate, non-nanoparticulate, etc.), and release profiles (e.g., immediate release, delayed release, sustained release, etc.) to provide therapeutic benefit with reduced side effects.
WO2007070986A1 Flavones The present invention relates to flavone compounds and their use in methods of treating or preventing parasitic infections, fungal infections and cell proliferative disorders. The present invention also relates to the use of flavone compounds in methods of controlling pests.
WO2008109055A8 Cyanopyrrole sulfonamides useful for modulation of the progesterone receptor In one embodiment, compounds of the following structure are described, wherein R1 to R7 are described herein. Formula (I). Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; treating or preventing uterine leiomyomata; treating or preventing endometriosis, dysfunctional bleeding, and polycystic ovary syndrome; treating or preventing hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms using the compounds described herein.
CN101868235A Compositions and methods for inhibiting the activation of dsRNA-dependent protein kinase and tumor growth inhibition The present invention relates to compositions and methods for preventing and treating a condition in a mammalian subject that include at least one inhibitor of double stranded RNA dependent protein kinase (PKR-I) prior to or concurrently with the treatment, wherein the treatment results to an inhibition of activation of dsRNA-dependent protein kinase. The compositions and methods of the present invention further include at least one potentiator that further enhances the inhibition of phosphorylation by PKR-I.
CN101134739A Novel beta-lactam compound and preparation method and chemical uses thereof The present invention relates to one kind of beta-lactam compound and its preparation process and medicinal use. The beta-lactam compound is 3-aryl-1-(n+2-aryl-n+2-hydroxy)alkyl-4- arylazacyclo butanoe, and has medicinal activity of regulating blood fat.
US20060035840 Beta-D-Glucopyranosyloxy)-3-(3-fluoro-4-methylbenzyl)-4,6-dimethylpyridine; sodium glucose co-transporter 2 (SGLT2) inhibitors; excellent hypoglycemic effect by excreting excess glucose into the urine through preventing the reabsorption of glucose at the kidney; antidiabetic agents; hyperglycemia The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 represents Nor CR1; X2 represents Nor CR2; X3 represents N or CR3; X4 represents N or CR4; and with the proviso that one or two of X1 to X4 represent N; R represents optionally substituted C3-8 cycloalkyl, optionally substituted C6-10 aryl, etc.; R1 to R4 represent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.
WO2010013987A2 Extraction method for increasing liquiritigenin content in glycyrrhizae radix et rhizoma or glycyrrhizae radix extract Disclosed herein is an extraction method for increasing liquiritigenin content in Glycyrrhizae Radix et Rhizoma or Glycyrrhizae radix extract, the method comprising: using water, an organic solvent, or a mixed solvent of water and the organic solvent to Glycyrrhizae Radix et Rhizoma to extract a product containing liquiritin (Step 1); and introducing water, an organic solvent, or a mixed solvent of water and the organic solvent into the product containing liquiritin extracted in Step 1, adding acid or base into the solution, and hydrolyzing the mixture to prepare a product containing liquiritigenin (Step 2).
WO2008055801A3 Antidiabetogenic calcium-peptide composition The invention relates to the use of a calcium-peptide composition obtained from at least one calcium salt, at least one caseinophosphopeptide (CPP), and/or at least one glycomacropeptide (GMP) for producing an agent for preventing and/or treating type II diabetes. Administering said composition makes it possible to significantly suppress the onset of type II diabetes (antidiabetogenic effect).
CN101735189A Preparation method, preparation and application of tricin The invention relates to a preparation method, preparation and application of botanical tricin. The preparation method of the tricin comprises the following steps of: performing ultrasonic extraction on plant materials by aqueous or non-aqueous organic reagents used as solvents; filtering extract, performing reduced pressure distillation and recycling solvents to obtain total extract; performing chromatographic separation; combining identical components; and performing purification treatment to obtain fine tricin. The obtained tricin has high purity, and the content of the tricin can reach above 98 percent. The method has the advantages of simplicity, feasibility, short extraction time, low cost, high yield and low energy consumption and is suitable for industrial production. The obtained tricin can be prepared into various preparation formulations by a pharmaceutical method. Screening experiments of antitumor bio-activities prove that the tricin has significant curative effect on resisting tumors and can be applied to the preparation of antitumor medicaments or medicament compounds.
US20110195949 2-benzothiophenyl- and 2-naphthyl-oxazolidinones and their azaisostere analogues as antibacterial agents The invention relates to antibacterial compounds of formula (I) wherein U, V, W, X, R1, R2, m, A, B and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament.
WO2011153157A2 Benzoquinolone inhibitors of vmat2 The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.Formula (I)
CN1853620A Fat emulsion of houttuynin analog A fatty emulsion with high stability and synergistic function contains houttuyninum analog, plant oil, phasphatide and the water for injection.
US20070071822 Film coated tablet for improved upper gastrointestinal tract safety A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.
US20110136781 Imidazotriazines and imidazopyrimidines as kinase inhibitors The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
CN1875975A Application of ocotillol type ginsenoside and its glucoside The invention relates the gen-seng ocotillo spooning and glycoside. The gen-seng ocotillo spooning and glycoside has good central stimulating action, so it can be used to prepare mental stimulant, health products, food additives and compound recipe preparation. It is mainly used to cure paroxysmal sleep and depression. It also can be used to cure proscenia, recover fatigue, improve memory, and modify emotion.
US20110136917 Tetrahydro-isoalpha acid compositions and methods for weight management Compositions and methods to promote or maintain weight loss utilizing tetrahydro-isoalpha acid compounds are disclosed. Methods to increase synthesis of GLP-1 are disclosed.
WO2006093041A1 Novel crystals of n-benzyl-n-ethyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9h-purin-9-yl)acetoamide An α-crystal, a Ϝ-crystal and a δ-crystal of N-benzyl-N-ethyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetoamide which are characterized by powder X-ray diffraction patterns and/or differential scanning calorimetry thermograms and have excellent thermal stability.
EP2534138A1 1,2,3-triazole-based peptidomimetic integrin inhibitors for the diagnosis and therapy of tumors The present invention refers to the field of chemical compounds bearing a 1,2,3-triazole ring of formula (I) and possessing guanidino and carboxylic groups or their isosteres, their preparation by Cu-catalyzed "click-chemistry", and medical - diagnostic use in pathologies where angiogenesis is altered, for example pathologic conditions of tumor origin, tumor metastasis, osteoporosis, and rheumatoid arthritis.
CA2149826C 7-glycosyloxybenzopyran derivative and antiallergic agent containing the derivative as active ingredient A 7-glycosyloxybenzopyran derivative represented by the following formula (see formula (I)) wherein, R1 is a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an alkenyl group or an aralkyl group, R2 is a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group or an aralkyl group and R3 is a glycosyl group whose hydroxyl group is protected or not protected, selected from the group consisting of glucosyl, mannosyl and galactosyl groups, and physiologically acceptable salts thereof.
US20080124367 50% by mass to 95% by mass of an oil constituent, which contains 10% by mass to 100% by mass of a solid or semisolid oil constituent, and 5% by mass to 50% by mass of particles; enhancing percutaneous absorption of a water-soluble agent A method of enhancing percutaneous absorption of a water-soluble agent comprises the steps of: applying a preparation for external use on skin, which preparation contains a water-soluble agent, onto skin, and applying an oil based composition for external use on skin onto the preparation for external use on skin, which preparation has been applied onto the skin. The composition contains 50% by mass to 95% by mass of an oil constituent, which contains 10% by mass to 100% by mass of a solid or semisolid oil constituent, and 5% by mass to 50% by mass of particles. The composition has occlusivity of at least 50%.
US7238489 Identification of sortase gene The present invention is a substantially purified sortase-transamidase enzyme from Gram-positive bacteria, such as Staphylococcus aureus. The enzyme having a molecular weight of about 23,539 daltons and catalyzing a reaction that covalently cross-links the carboxyl terminus of a protein having a sorting signal to the peptidoglycan of a Gram-positive bacterium, the sorting signal having: (1) a motif of LPX3X4G (SEQ ID NO: 37) therein; (2) a substantially hydrophobic domain of at least 31 amino acids carboxyl to the motif; and (3) a charged tail region with at least two positively charged residues carboxyl to the substantially hydrophobic domain, at least one of the two positively charged residues being arginine, the two positively charged residues being located at residues 31-33 from the motif, wherein X3 is any of the twenty naturally-occurring L-amino acids and X4 is selected from the group consisting of alanine, serine, and threonine, and wherein sorting occurs by cleavage between the fourth and fifth residues of the LPX3X4G (SEQ ID NO: 37) motif. Variants of the enzyme, methods for cloning the gene encoding the enzyme and expressing the cloned gene, and methods of use of the enzyme, including for screening for antibiotics and for display of proteins or peptides on the surfaces of Gram-positive bacteria, are also disclosed.
CN1626109A Substance of poly pentenol capsule and its prepn. method A polypentenol capsule containing oil polypentenol (1-20 wt.%) and plant oil (20-95 wt.%). It is prepared from the ointment containing polypentanol through vacuum molecular distilling, vacuum molecular distilling of the residue to obtain oily polypentenol, and proportionally mixing it with plant oil.
CN102627654A Human immunodeficiency virus (HIV)-1 protease inhibitors containing isosorbide structural units and preparation method and application thereof The invention relates to human immunodeficiency virus (HIV)-1 protease inhibitors containing isosorbide structural units and a preparation method and application thereof, which belong to the field of chemical drugs. A compound has a structure like a general formula 1. The preparation method comprises adopting an amino chiral alcohol compound to serve as a raw material, enabling the compound to react with isosorbide with hydroxyl activated by chloroformic acid p-nitrophenol ester, and a series of HIV-1 protease inhibitors containing isosorbide structures are synthesized through direct synthesis or further through functional group transformation. Compounds of the HIV-1 protease inhibitors can inhibit protease activity and can be used for preparing an anti-aids drug.
EP1673087A2 Alkoxy substituted imidazoquinolines Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
WO2009148287A3 Novel α-iso-cubebene compound extracted from schisandra chinensis and composition containing the compound as active ingredient for preventing and treating inflammatory diseases The present invention relates to a novel α-iso-cubebene compound which is extracted from Schisandra chinensis. As a result of using a TNF-α-stimulated HUVEC model, the extracted novel α-iso-cubebene compound has been proven to effectively suppress the generation of ROS, the expression of VCAM-1 and E-selectin, the activation of NF-B transcription factor and monocyte adhesion to endothelial cells. Especially, while the α-iso-cubebene suppresses TNF-α-induced expression of VCAM-1 and E-selectin which perform a pivotal role in in-vitro model of early atherogenesis, it does not change the expression of ICAM-1. In addition, during early atherogenesis, a cytokine such as TNF-α activates membrane-bound NADPH oxidase and stimulates intracellular ROS generation. Then, the cytokine activates an oxidation/reduction-sensitive transcription pathway such as NF-B and induces the expression of endothelial adhesion molecules. Since the α-iso-cubebene reduces the generation of ROS and suppresses the activation of oxidation/reduction-sensitive transcription factor NF-B, it suppresses TNF-α-stimulated VCAM-1 expression and monocyte adhesion to endothelial cells. Therefore, the α-iso-cubebene provides a composition for preventing and treating inflammation.
EP2493471A1 Novel enteric combination therapy There is disclosed herein a composition for treating gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhoea, chronic idiopathic nausea, IBD-associated constipation and diarrhoea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the composition comprising: (i) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or ( (ii) at least one anti-clostridial agent selected from the above combined with an opioid blocking agent. There is also disclosed herein a method of treating various gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhoea, chronic idiopathic nausea, IBD-associated constipation and diarrhoea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the method comprising administering orally, via enema or by suppository: (i) a composition of the invention; (ii) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (iii) at least one anti-clostridial agent selected from the above and an opioid blocking agent to a patient in need of such treatment.
EP2585469A1 Benzodioxole or benzodioxepine heterocyclic compounds phosphodiesterase inhibitors Compounds of the general formula (I) wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, -S(O)- and - S(0)2-; R3 is -CHF2, -CF3, -OCHF2, -OCF3, -SCHF2 or -SCF3; X is a bond, -CH2-, or -NH-; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.
CN103611045A Composition for treating rumen indigestion of beef cattle The invention provides a composition for treating rumen indigestion of beef cattle, which comprises 10-30g of Fructus Forsythiae, 8-25g of phellodendron bark, 5-15g of rhubarb, 8-25g of hawthorn, 10-30g of picrorhiza rhizome, 7-20g of mirabilite, 5-15g of alcoholic rhizoma anemarrhenae, 5-15g of retinervus luffae fructus, 8-25g of medicated leaven, 8-25g of moleplant seed, 8-25g of fructus aurantii, 8-25g of dried orange peel, 8-25g of bush-cherry seed, 15-50g of honied radix astragali, 10-30g of dangshen, 10-30g of amomum fruit, 8-25g of pawpaw, 10-20g of tuckahoe, 7-20g of agilawood, 7-25g of Chinese yam, 7-25g of figwort and 10-20g of licorice. The composition is simple in proportioning and convenient to use, and is used for clearing away heat and toxic material, activating blood circulation to dissipate blood stasis, promoting circulation of qi and to relieve pain, strengthening the spleen, stimulating the appetite, strengthening the middle-jiao, invigorating qi, removing heat from the blood and promoting salivation.
US20120040924 Purine nucleoside monophosphate prodrugs for treatment of cancer and viral infections The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV in human patients or other animal hosts. The compounds are certain 6-substituted purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1, HIV-2, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV.
WO2014053650A1 Use of masitinib for treatment of cancer in patient subpopulations identified using predictor factors The present invention relates to a method for treating patients afflicted with cancer, wherein said patients are treated with a tyrosine kinase inhibitor, mast cell inhibitor or c-Kit inhibitor, in particular masitinib, optionally in combination with at least one antineoplastic agent. The tyrosine kinase inhibitor, mast cell inhibitor or c-Kit inhibitor, and the optional at least one antineoplastic agent, are administered in a dosage regimen that comprises a therapeutically effective amount. The present invention also relates to methods for predicting therapeutic response to said treatment in a given patient and therefore identification of applicable patient subpopulations based upon these predictor factors; sometimes referred to as biomarkers. One method is based upon the clinical marker of pain intensity. The second method is based upon gene expression predictive biomarkers assessed via RNA expression in peripheral blood cell samples collected prior to treatment with a compound of the invention (i.e. a tyrosine kinase inhibitor, mast cell inhibitor or c-Kit inhibitor, especially masitinib). Advantageously, the present invention relates to a method for treating patients afflicted with pancreatic cancer wherein said patients are treated with a tyrosine kinase inhibitor, mast cell inhibitor or c-Kit inhibitor, and in particular masitinib, optionally in combination with at least one antineoplastic agent, and in particular gemcitabine.
CN1809353B Medicine for prevention of and treatment for arteriosclerosis and hypertension. Disclosed is the medicine used for preventing and treating arteriosclerosis, hypertension, heart disease or cerebrovascular disease. The composition of the medicine comprises (A) angiotensin II receptor antagonist which is selected from the compounds with the general formula (I) and is composed of ester which has pharmacological acceptance property and salt which has pharmacological acceptance property (such as olmesartan medoxomil) and (B) calcium channel blocker which is used as the active constituent and is selected from the dihydro-pyridine derivatives and is composed of salt which has which has pharmacological acceptance property.
CN1795877A Ganoderma lucidum capsule of lycopene A medicine in the form of capsule for regulating immunity, suppressing tumor and delaying sanility is proportionally prepared from lycopene, ganoderma spore powder or refined ganoderma powder, auxiliary and VE.
CA2532596C Anti-inflammatory formulations The invention features compositions and methods for reducing inflammation of ocular tissue by administering to an individual a mixture of ingredients containing carotenoid and a polyphenol compound.
WO2005002551A3 Vanilloid receptor (vr) 1 inhibitors for treatment of human immunodeficiency virus (hiv)-mediated pain states The invention relates to the application of Vanilloid receptor (VR) 1 inhibitors for drug development and for the treatment of HIV-mediated neuropathies and neuropathic pain states. Further, the inventor identified a novel signaling cascade connecting the HIV receptor CXCR4 to VR1. Thus, the invention provides molecular evidence that HIV-mediated pain states - initiated upon binding of the virus to CXCR4 - can be inhibited by VR1 antagonists blocking the final execution of the CXCR4/VR1 pathway. In addition, the invention demonstrates that present standard therapies for HIV-mediated pain (which do not include VR1 inhibitors) can not interfere with the CXCR4/VR1 pathway thus explaining inefficient patient treatment in the clinics.
WO2013177226A1 Systems for treating pulmonary infections Provided herein are systems for treating a subject with a pulmonary infection, for example, a nontuberculous mycobacterial pulmonary infection, a Burkholderia pulmonary infection, a pulmonary infection associated with bronchiectasis, or a Pseudomonas pulmonary infection. The system includes a pharmaceutical formulation comprising a liposomal aminoglycoside dispersion, and the lipid component of the liposomes consist essentially of electrically neutral lipids. The system also includes a nebulizer which generates an aerosol of the pharmaceutical formulation at a rate greater than about 0.53 gram per minute. The aerosol is delivered to the subject via inhalation for the treatment of the pulmonary infection.
US20110288147 Compositions and methods for the specific inhibition of gene expression by DSRNA containing a tetraloop The invention features compositions and methods that are useful for reducing the expression or activity of a specified gene in a eukaryotic cell.
WO2010127452A1 5-oxo-ete receptor antagonist compounds The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.
US20100047178 Perylenequinone derivatives and uses thereof The present invention relates to compounds which are perylenequinone derivatives, their stereoisomers and atropisomers. These compounds can be particularly useful as photosensitizers or sononsensitizers in photodynamic or sonodynamic therapy. The invention also relates to various methods for using these compounds in photodynamic and/or sonodynamic therapy. The compounds also are useful as therapeutic agents for treating various hyperproliferative disorders.
CN103239400A Itraconazole nano-suspension and preparation method thereof The invention belongs to the technical field of medicines, and discloses an itraconazole nano-suspension and a preparation method thereof. Itraconazole is low in water solubility and oral bioavailability, so that the popularization and the use of the itraconazole are limited. The itraconazole nano-suspension is characterized by comprising the itraconazole, copovidone PVPS630 and povidone PVPK-90 in the mass ratio of (4-10): (1-2): (1-2). The nano-suspension preparation method needs mild conditions, is simple and controllable, and ensures that the itraconazole can achieve relatively high oral bioavailability.
WO2009098369A1 Antimitotic compounds derived from vinca alkaloids, preparation thereof and therapeutic use thereof The invention relates to novel derivatives of the vinblastine and vinflunine family, substituted in the 12’-position of formula (A), and also to the method for the production thereof. The invention also relates to the use of these compounds or of salified forms thereof for the treatment of cancerous diseases.
CN101318952A Sigma Acceptor activator compound and uses thereof The invention discloses a medicine for treating or preventing the mood disorder of a sufferer who experiences or is easy to suffer from the mood disorder. The medicine comprises a monomer compound or a composition; the monomer compound or the composition comprises a triarylated lupetazin compound with the following formula; and the triarylated lupetazin compound has a chemical structural formula as shown in general formula (I).
US20080145410 An iron-containing complex to treat hyperphosphatemia by adsorbing excess phosphates in the blood; capacity of >140 mg adsorbed phosphate by 1 g complex of an insoluble carbohydrate (starch), polynuclear iron oxide/hydroxide and a soluble glucose; stability; packaging; industrial scale The present invention relates to a new iron containing phosphate adsorbent and its use e.g. for treating hyperphosphataemia.
WO2004071427A3 Screening and treatment methods for prevention of preterm delivery Provided herein are methods, combinations, and kits for screening and treating a subject. In practicing the methods a sample, such as urine, blood, plasma, saliva, cervical fluid, vaginal fluid, or a tissue sample, is obtained from a subject; if the level of a marker, such as a fetal restricted antigen or estriol, is indicative of a risk of imminent or preterm delivery, a progestational agent is administered to the subject. By virtue of administration of the agent delivery can be delayed.
WO2014087230A1 Use of eribulin in the treatment of breast cancer The invention provides methods of treating breast cancer in subjects having locally advanced or metastatic breast cancer.
CN101129370A Rimonabant or its salt dispersion patch capable of using in medicine and method of producing the same The invention provides a dispersible medicinal tablet which comprises rimonabant, its medicinal salts and medicinal carriers, wherein the medicinal carriers include one or more selected from crumbling agent, bulking agent, surface active agent, wetting and bonding agent, and lubricating agent. The tablet is prepared through wet method granulation and pelleting, the surface active agent can improve the water non-insolubility and non-wettability of rimonabant and its medicinal salts, the bioavailability of the medicament can thereby be improved.
CN102218040A Oral disintegrating tablets of microcrystallites of aripiprazole composition and preparation method thereof The invention relates to orally disintegrating tablets of microcrystallites of an aripiprazole composition and a preparation method thereof, and the orally disintegrating tablets mainly compose the microcrystallites of the aripiprazole lactose composition, a filling agent, a disintegrating agent, a flavor correction agent and a lubricating agent, wherein the particle size of the microcrystallites of the aripiprazole lactose composition is less than 30 mu m. The preparation method comprises the following steps: uniformly mixing all components of the aripiprazole orally disintegrating tablets and then directly tabletting or performing wet-granulation tabletting. The microcrystallites obtained by common micronization of the aripiprazole lactose composition are higher in dissolution rate in comparison with those by independent micronization of aripiprazole; simultaneously, the crystal form of the aripiprazole in the microcrystallites of the composition is not transformed and the uniformity of content of the orally disintegrating tablets is higher; and the hardness of the aripiprazole orally disintegrating tablets is 5-8kg, the disintegration time limit is less than 30 seconds, not only the tablets can be prevented from breaking during transportation, but also the tablets are convenient to take.
WO2010021149A1 Spiro compound capable of inhibiting acid secretion Disclosed is a novel prophylactic/therapeutic agent for digestive system diseases. The prophylactic/therapeutic agent for digestive system diseases comprises a compound represented by the formula or a salt or prodrug thereof. In the formula, the ring A represents a 5- to 7-membered nitrogenated hetero ring which may have a substituent; the ring B represents a 5- to 6-membered aromatic ring which may have a substituent; Ar represents an aromatic ring group which may have a substituent; L represents a C1-4 alkylene which may have a substituent, or –SO2-; X and Y independently represent a carbon atom which may have a substituent, a nitrogen atom which may have a substituent, an oxygen atom, or a sulfur atom which may be oxidized, provided that, when X and Y independently represent a carbon atom which may have a substituent or a nitrogen atom which may have a substituent, the substituent in X and the substituent in Y may together form a ring; and m represents an integer of 0 to 2.
USRE39574 Quinazolinone containing pharmaceutical compositions for prevention of neovascularization and for treating malignancies The invention provides a composition for attenuating neovascularization and treating malignancies, including a pharmaceutically effective amount of a compound having a formula: wherein: R1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl and lower alkoxy; R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy, and R3 is a member of the group consisting of hydrogen and lower alkenoxy carbonyl; as active ingredient therein, in combination with a pharmaceutically acceptable carrier.
US20120283199 Neuroprotective ganglioside compositions for use in treating or diagnosing huntington's disease Huntington's disease (HD) is a neurodegenerative disorder caused by the expansion of a polyglutamine stretch in the protein huntingtin (Htt). HD neurons are dysfunctional at multiple levels and have increased susceptibility to stress and apoptotic stimuli. As described therein there is provided compound(s), composition(s), methods and/or kits for the treatment and/or diagnosis of Huntington's disease.
WO2010108410A1 Use of catechin in preparation of retrovirus integrase inhibitor Use of catechin in preparation of retrovirus integrase inhibitor. The retrovirus integrase inhibitor can treat AIDS caused by retrovirus HIV, the adult T-cell leukemia, tropical spastic paraparesis or HTLV-I-associated myelopathy caused by HTLV, and lymphoid leukosis, erythroblastosis, myeloblastosis, myelocytoma, avian sarcoma, endothelioma, nephroblastosis, fibrosarcoma and osteopetrosis caused by avian sarcoma and/or leukosis virus. The retrovirus integrase inhibitor has high therapeutic efficacy, low cost and low toxicity and side effects.
US20100330082 Nlrr-1 antagonists and uses thereof NLRR-1 antagonists and methods of their use in treating cancer and other disorders are provided.
WO2008102888A1 Novel pseudoglycolipid and use thereof Disclosed is a novel pseudoglycolipid useful for treatment of cancers and the like. Also disclosed are a novel synthesis intermediate of such a novel pseudoglycolipid, and a pharmaceutical product and the like containing such a novel pseudoglycolipid. Specifically disclosed is a compound represented by the general formula (1) below or a salt thereof. (In the formula, the symbols are as defined in the description.)
WO2012011741A3 Novel fusarisetin compounds, and use thereof The present invention relates to novel fusarisetin compounds separated from Fusarium sp. FN080326 and having an anticancer activity, and to the use thereof. In detail, novel fusarisetin compounds separated and purified from Fusarium sp. FN080326, which is in turn separated from a soil sample, have an inhibitory activity on the proliferation and transfer of cancer cells such as breast-cancer cells, liver-cancer cells or myeloid-leukemic cells. Therefore, the compounds can be effectively used for anticancer compositions containing the compounds as active ingredients.
WO2006117371A1 4-PHENYL-5-0X0-l,4,5,6,7,8-HEXAHYDR0QËIN0LINE DERIVATIVES AS MEDICAMENTS FOR THE TREATMENT OF INFERTILITY The present invention- relates to 2-methyl-4-phenyl-5-oxo-1 ,4,5,6,7,8-hexahydroquinoline derivatives having the general Formula (I) wherein the substituents are defined as in the description, or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 2-methyl-4-phenyl-5-oxo-1 ,4,5,6,7,8-hexahydroquinoline derivatives in therapy, more specifically for the treatment of fertility disorders.
US20090203713 Hedgehog pathway antagonists to treat disease Compounds, compositions, kits and methods for modulating hedgehog pathway activity, and treating conditions related to abnormal or aberrant hedgehog pathway activity, are disclosed.
US20120101102 Method for predicting therapeutic effect of chemotherapy on renal cell cancer The present invention developed a novel antitumor agent for renal cell carcinoma that cannot be fully treated by the existing therapies. The present invention provides an antitumor agent comprising a combination drug of tegafur/gimeracil/oteracil potassium that ensures an excellent therapeutic effect in renal cell carcinoma patients that is superior to that of the existing therapies, by way of selecting the patients based on thymidylate synthase.
WO2012028874A1 Cytotoxic luminescent metal complexes The invention provides new antineoplastic agents comprising mono-nuclear complexes containing a tetrapyrido[3,2-a:2',3'-c:3'',2''-h:2''',3'''-j]phenazine, tpphz, ligand, these complexes have dual functioningimaging/therapeutic properties. Also described is their use in photodynamic therapy and as chemotherapeutic agents having cytotoxicity comparable to the platinum-based chemotherapeutics and their use especially for platinum-resistant tumour cells.
CN103690525A Application of Artoxanthochromane in preparation of medicine for treating tongue cancer The invention discloses application of Artoxanthochromane in preparation of a medicine for treating tongue cancer and belongs to the technical field of novel application of medicines. In vitro MTT ((3-4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anti-tumor activity evaluation discovers that Artoxanthochromane has a remarkable inhibition effect on the growth of human tongue cancer cell line PTca8113 and T6. Therefore, Artoxanthochromane can be used for preparing a tongue cancer resistance medicine and has an excellent developing application prospect. The application of Artoxanthochromane in preparation of the medicine for treating tongue cancer is disclosed for the first time, and Artoxanthochromane has a strong inhibition activity to tongue cancer cells, and remarkable progress is obtaine.
CN101088509A Nutritious health oral liquid of lily polysaccharide The present invention relates to health product technology, and provides one kind of nutritious health oral liquid of lily polysaccharide. The nutritious health oral liquid with lily polysaccharides as the main active components contains lily polysaccharide PS-W 2-30 wt%, lily polysaccharide PS-L 0.1-10 wt%, lily alkaloid 0.01-1.0 wt%, and seasonings 0.01-5 wt%. The nutritious health oral liquid has the functions of regulating immunity, resisting oxidation, resisting senility, reducing blood sugar, etc, and possesses health care and auxiliary disease treating effects.
US8497300 Arsenic therapy for APLS-type autoimmune lymph-oproliferative syndrome in mice and humans The invention relates to the use of an arsenic compound for the preparation of a medicament that is used to treat autoimmune diseases.
US6930098 Polysulphated cyclodextrins or addition salts thereof in obtaining pharmaceutical compositions for use in the treatment of arthrosis. The present invention relates to the method of using polysulphated cyclodextrins or addition salts thereof for use in the treatment of arthrosis, and pharmaceutical compositions thereof.
CN101283983A Stable camptothecine liposome composition A stable liposome composition comprises camptothecin or derivatives thereof, phospholipid, cholesterol, organic acids and the buffer salts of the camptothecins, and pharmaceutically-acceptable excipient. The composition can specifically increase the stability of the camptothecins, improve the curative effect, and reduce the toxic and side effects of the camptothecins.
CN101538258A New composition of salvia miltiorrhiza and derivative, preparation method and medicine application thereof The invention relates to a new composition of salvia miltiorrhiza and a derivative, a preparation method and application thereof, belonging to the technical field of medicine, wherein the three compositions are salvia miltiorrhiza new lactone A, salvia miltiorrhiza new lactone B and salvia miltiorrhiza new lactone C and derivative thereof and effective parts, which have a (1) chemical structure general formula. The invention also relates to application of a new skeleton composition and a derivative and an effective part thereof on preparing medicine, in particular to the application of same on preparing spiritual class medicine and anticancer class medicine, wherein R1 is selected from hydrogen, alkyl, undersaturated alkyl, hydroxide radical, alkoxyl, carboxyl, esterifiable carboxyl, balmy substituent, halogen, and the like, R2, R3 and R4 are selected from hydrogen, alkyl, undersaturated alkyl, balmy substituent, low grade sugar indican, polysaccharide indican, metallic ions and organic acid ester group, and the R2, the R3 and the R4 can be same and also can be different.
CN1781548A Medicinal preparation for treating stomach and intestine diseases and its preparing method The medicinal preparation for treating gastrointestinal diseases is prepared with berberine hydrochloride, chlorphenamine maleate, thiamine nitrate, protein tannate, ethacridine lactate, aluminum silicate, starch, magnesium stearate and alcohol. It is used in treating dysentery, acute and chronic gastroenteritis, acute and chronic diarrhea, abnormal fermentation inside intestine, etc. Compared with available the technology, the present invention has the advantages of high curative effect, no toxic side effect, taking safety, etc.
WO2011031350A1 Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof A method of providing a patient with controlled release of ketone-containing opioid using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing the ketone-containing opioid is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of the ketone-containing opioid from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.
CN103356742A Emulsifiable paste for treating skin disease and formula thereof The invention discloses an emulsifiable paste for treating skin disease and a formula of the emulsifiable paste. According to the formula, the emulsifiable paste comprises the following components: 4-5g of camphor, 3-6g of menthol, 12-14g of benzoic acid, 6-8g of salicylic acid, 1-2g of zinc oxide, 3-4g of sublimed sulfur, 1-2g of methyl salicylate, 1-2g of borneol, 0.3-0.5g of glycyrrhetinic acid, 0.2-0.4g of chlorhexidine gluconate and 1-1.5g of diphenhydramine. The preparation process comprises the following steps of: first, grinding camphor, menthol and borneol into fine powder; then, adding benzoic acid, salicylic acid, zinc oxide, sublimed sulfur, methyl salicylate, glycyrrhetinic acid, chlorhexidine gluconate and diphenhydramine and grinding into paste; and packaging by using small containers for later use. The emulsifiable paste disclosed by the invention is simple to prepare and has the advantages of reliable curative effect, high economic value and high utilization ratio.
US7704951 administering as an active ingredient selenoprotein P and/or a peptide fragment or a series of peptide fragments derived from said protein; suitably applicable to diseases with decrease in motor function A novel medicament for treating neurodegenerative diseases, especially for ameliorating dyskinesia, comprising as an active ingredient selenoprotein P and/or a peptide fragment or a series of peptide fragments derived from said protein is provided. The novel medicament for treating neurodegenerative diseases, especially for ameliorating dyskinesia, according to the present invention is suitably applicable to diseases with decrease in motor function.
US7390781 Methods of using truncated glial cell line-derived neurotrophic factor Disclosed are novel proteins, referred to as truncated glial cell line-derived neurotrophic factor (truncated GDNF) proteins, that promote dopamine uptake by dopaminergic cells and promote the survival of nerve cells. Also disclosed are processes for obtaining the truncated GDNF proteins by recombinant genetic engineering techniques.
US20100190750 GPR119 Receptor Agonists in Methods of Increasing Bone Mass and of Treating Osteoporosis and Other Conditions Characterized by Low Bone Mass, and Combination Therapy Relating Thereto The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.
CN101850119B Compound preparation used for treating melancholia and senile dementia The invention discloses a compound preparation used for treating depression and senile dementia. The compound preparation comprises the following components in part by weight: 1 part of rolipram and 0.25 to 200 parts of antiemetic medicament, wherein the antiemetic medicament is granisetron, ondansetron, tropisetron, aprepitant or metoclopramide. The compound preparation is prepared from the rolipram and the granisetron, the ondansetron, the tropisetron, the aprepitant or the metoclopramide. The compound preparation has an effective curative effect of treating the melancholia and the senile dementia, and simultaneously solves the technical problems that in the prior art, the rolipram causes adverse reactions such as vomition, sicchasia, headache and the like.
US20090131509 Aminoacid Derivatives Containing a Disulfanyl Group in the form of Mixed Disulfanyl and Aminopeptidase N Inhibitors The invention relates to novel compounds of formula (I): H2N—CH(R1)—CH2—S—S—CH2—CH(R2)—COONH—R5, wherein R1 is a hydrocarbon chain, phenyl or benzyl radical, methylene radical substituted by a 5 or 6 atom heterocycle; R2 is a phenyl or benzyl radical, a 5 or 6 atom aromatic heterocycle, methylene group substituted by a 5 or 6 atom heterocycle; R5 is a CH(R3)—COOR4 radical, wherein R3 is hydrogen, an OH or OR group, a saturated hydrocarbon group, a phenyl or benzyl radical and OR4 is hydrophile ester, or 5 or 6 membered heterocycle comprising several heteroatoms selected from a group consisting of nitrogen, sulphur and oxygen, with at least two nitrogene atoms, wherein said heterocycle is substitutable by an alkyl C1-C6, phenyl or benzyl radical. The use of the inventive compounds in the form of drugs, a pharmaceutical composition comprising said compounds, a pharmaceutically acceptable excipient, the use in conjunction of at least one type of cannabinoid derivative for potentiating the analgesic and antidepressant effect of the novel compounds of formula (I) and/or morphine or the derivatives thereof are also disclosed.
WO2011019821A2 METHOD FOR MAKING 3α-HYDROXY, 3β- METHYL-5α-PREGNAN-20-ONE (GANAXOLONE) Applicants have discovered a method for the stereoselective and regioselective synthesis of 3α-hydroxy, 3β-methyl-5α- pregnan-20-one (ganaxolone) comprising reacting 5α-pregnane-3,20-dione; with an organometallic methylating agent in an inert solvent to provide a compound of the formula.
CA2261835C Long-acting drugs and pharmaceutical compositions comprising them Prodrugs and pharmaceutically acceptable salts thereof are provided carrying functional groups sensitive to mild bases and capable of slowly hydrolyzing to the original active drug molecule under physiological conditions. The prodrugs are preferably of the formula X - Y wherein Y is a moiety of a drug bearing at least one functional group selected from free amino, carboxyl, hydroxyl and/or mercapto, and X is a radical selected from radicals of formulas (i) to (iv) wherein R1 and R2, the same or different, are each hydrogen, alkyl, alkoxy, alkoxyalkyl, aryl, alkaryl, aralkyl, halogen, nitro, sulfo, amino, ammonium, carboxyl, PO3H2, or OPO3H2; R3 and R4, the same or different, are each hydrogen, alkyl or aryl; and A is a covalent bond when the radical is linked to a carboxyl or mercapto group of the drug Y, or A is OCO- when the radical is linked to an amino or hydroxyl group of Y, and pharmaceutically acceptable salts thereof. Examples of such prodrugs are those wherein Y is a moiety of insulin, human or bovine growth hormone, antibiotics, propanolol and others.
CN102018701B Pharmaceutical application of angle flavonol lignans to preparing glucosidase inhibitors The invention relates to application of angle flavonol lignans to preparing glucosidase inhibitors, in particular to application of B-ring dioxane angle flavonol lignans or pharmaceutically acceptable salts thereof to preparing drugs for inhibiting alpha-glucosidase and preventing and treating type II diabetes mellitus. The flavonol lignans have extremely obvious activity for inhibiting alpha-glucosidase and the intensity of activity of the flavonol lignans for inhibiting alpha-glucosidase has reached 66.7% at the concentration of 40mcg/ml. The measured half-inhibitory concentration of the flavonol lignans shows that the intensity of activity of the flavonol lignans for inhibiting alpha-glucosidase is 4.4 times that of the positive control drug acarbose. The pharmacodynamics result shows that the flavonol lignans or pharmaceutically acceptable salts thereof can be expected to be applied to preparing glucosidase inhibitors, especially the drugs for preventing and treating type II diabetes mellitus, namely non-insulin dependent diabetes mellitus.
US7153862 αv integrin receptor antagonists The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αvβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
CN103214488A Quinolinone derivative, pharmaceutical composition by taking quinolinone derivative as active component and preparation method The invention discloses a quinolinone derivative, a pharmaceutical composition by taking the quinolinone derivative as an active component and a preparation method, a general formula of the quinolinone derivative is:, the invention also relates to the preparation method of the quinolinone derivative, and the pharmaceutical composition by taking the quinolinone derivative as the active component.
US20100292159 Method of treatment or prophylaxis of inflammatory pain This invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory conditions.
US7850971 PSMA antibodies and protein multimers The invention includes antibodies or antigen-binding fragments thereof which bind specifically to conformational epitopes on the extracellular domain of PSMA, compositions containing one or a combination of such antibodies or antigen-binding fragments thereof, hybridoma cell lines that produce the antibodies, and methods of using the antibodies or antigen-binding fragments thereof for cancer diagnosis and treatment. The invention also includes oligomeric forms of PSMA proteins, compositions comprising the multimers, and antibodies that selectively bind to the multimers.
US7002019 aryl hydrocarbon; oxidation of 4,5-dihydro-1,3-azoles to fully unsaturated ring; heterocyclic ketones A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.
US20110301236 HeLa-C3 Apoptosis Inducer from Garcinia paucinervis A novel compound isolated from the plant Garcinia paucinervis. The compound's structure is as follows: The compound possesses a potent ability to activate caspase-3 in HeLa-C3 cells within 72 h at a low concentration of 25 μM. The IC50 on HeLa cells for this compound was measured to be below 10 μM, indicating a strong HeLa cell growth inhibitory effect.
CN103405464A Medicine for treating respiratory system infection of livestock and poultry The invention relates to a medicine for treating respiratory system infection of livestock and poultry, and aims at providing synergism compound tylosin tartrate for livestock injection. The medicine has rapid and accurate treatment effects on respiratory system infection and complications of livestock and poultry. The medicine is prepared from the following ingredients in parts by weight: 1 part of tylosin tartrate, 1 part of kanamycin sulfate, 0.2 part of trimethoprim, 0.2 part of a cosolvent and 0.05-0.1 part of a pain reliever, wherein the cosolvent is citric acid, succinic acid or a compound of the two, and the pain reliever is procaine hydrochloride, lidocaine hydrochloride or a compound of the two. The synergism compound tylosin tartrate for livestock injection provided by the invention contains three components, namely the tylosin tartrate, kanamycin sulfate and trimethoprim; the problem that secondary infection cannot be well controlled due to the narrow antibacterial spectrum of the tylosin tartrate when mycoplasma infection is treated can be solved; the problem that the trimethoprim is poorly soluble in water can be solved, and a synergism effect of the tylosin tartrate and kanamycin sulfate can be achieved; the dosage is accurate, and the use is convenient.
US20120027854 Pharmaceutical composition comprising ezetimibe and simvastatin The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing dosage forms containing simvastatin and ezetimibe, comprising the steps of providing a first composition containing simvastatin, providing a second composition containing ezetimibe, and forming a dosage form comprising at least two separate compartments, wherein one compartment is formed using either the first or the second composition and another compartment is formed using the other composition. The present invention also relates to a process for preparing dosage forms containing simvastatin and ezetimibe, wherein the process involves a direct compression step. Furthermore, the present invention belongs to a dosage form obtained by this process, comprising at least two separate compartments, wherein one compartment contains simvastatin and one compartment contains ezetimibe. Finally, the present invention relates to a combination dosage form comprising a combination of simvastatin and ezetimibe present in two separate compartments of the dosage form.
EP2785328A1 Novel slow-releasing ophthalmic compositions comprising povidone iodine The present invention provides novel slow-releasing ophthalmic compositions containing Povidone Iodine (PVP-I) and uses thereof in the treatment of acute infections of at least one eye tissue from bacterial, mycobacterial, viral, fungal, or amoebic causes and for preventing such infections in appropriate clinical settings. Each of the ophthalmic compositions contains povidone iodine, osmotic pressure regulator, suspending agent and EDTA-Na, wherein povidone iodine exists as microsphere particles formed by PVP-I and sodium alginate.
US7575923 CD19xCD3 specific polypeptides and uses thereof Described are novel single-chain multifunctional polypeptides comprising at least two binding sites specific for the CD19 and CD3 antigen, respectively. Further provided are polypeptides, wherein the above-described polypeptide comprises at least one further domain, preferably of pre-determined function. Furthermore, polynucleotides encoding said polypeptides as well as to vectors comprising said polynucleotides and host cells transformed therewith and their use in the production of said polypeptides are described. In addition, compositions, preferably pharmaceutical and diagnostic compositions are provided comprising any of the afore-described polypeptides, polynucleotides or vectors. Described is also the use of the afore-mentioned polypeptides, polynucleotides and vectors for the preparation of pharmaceutical compositions for immunotherapy, preferably against B-cell malignancies such as non-Hodgkin lymphoma.
US20080090865 Non-insulin dependent diabetes; agonists of G-protein coupled receptor 40 (GPR40); for example, 3-(indan-1-yloxy)-8-(oxazolidin-2,4-dion-5-yl)-5,6,7,8-tetrahydroquinoline Bicyclic compounds containing a fused pyridine ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
US6867230 Antibacterial and antiprotozoal agents This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R10 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of treating bacterial and protozoal infections by administering the compounds of formula 1.
CN1931197A Health product and medicine containing glossy ganoderma and selenium The health product and medicine consists of glossy ganoderma and selenium mainly, and may be used to raise body's immunity and resist various kinds of diseases. Of the product of the present invention, each daily taken unit for adult includes glossy ganoderma in 0.15-15000 mg and selenium in 0.004-400 mcg.
EP2255807A1 Method of treating sleep disorders using the combination of eplivanserin and zolpidem The instant invention relates to a method of treating sleep disorders by using eplivanserin or pharmaceutically acceptable salts or esters thereof and zolpidem by evaluating the effect of eplivanserin combined with the sleep-inducing agent zolpidem on psychomotor/cognitive performance.
CN1833671A Paste for relieving mammary gland gall A Chinese-medicine in the form of ointment for treating mammary cancer, mastoplasia, mammary phyma, mastitis, mastofibroma, thynoma, periomethritis, ischias, etc is prepared from sesame oil and 6 Chinese-medicinal materials including safflower, cinnamon bark, Chinese angelica root, etc. through grinding, heating in oil, filtering, adding minium and concentrating.
WO2012095509A8 Composition for accelerating alcohol metabolism and for reducing the risk of alcohol induced diseases The present invention refers to a liquid composition comprising Vitamin C, L-glutamine and/or L-glutamic acid, L-cysteine and/or L-cystine, riboflavin, succinic acid, fumaric acid, coenzyme Q 10, niacin and hydrogen carbonate, phosphate or any other buffering system, in particular for use as a food composition, dietary or food supplementation, and pharmaceutical composition, respectively. The present invention refers further to the composition according to the invention for use in the treatment and/or prophylaxis of neuropathy, neurodegenerative diseases including late-onset Alzheimer´s disease, tumour metastasis and cancer, in particular of pancreatic, esophageal, oropharyngolaryngeal, liver, colorectal, lung and/or breast cancer.
CA2474280C Compositions containing alpha-2-adrenergic agonist components Compositions useful for improving effectiveness of alpha-2-adrenergic agonist components include carrier compo-nents, alpha-2-adrenergcic agonist components, solubility enhancing components which aid in solubilizing the alpha-2-adrenergic agonist components. Tn one embodiment, the alpha-2-adrenergic agonist components include alpha-2-adrenergic agonists In an-other embodiment, the solubility enhancing components include carhoxymethylcellulose.
CN102861078A Application of Houttuynoid D in medicine for treating prostatic cancer The invention discloses application of Houttuynoid D in preparation of a medicine for treating prostatic cancer, belonging to the technical field of new application of medicine. The invention discovers that Houttuynoid D has the remarkable inhibitory effects on the growth of human prostatic cancer cell strains, including ALVA, gpc-1, 9L-B and Du145 through the evaluation of in-vitro MTT antineoplastic activity. Therefore, Houttuynoid D can be used for preparing the anti-prostatic cancer medicine and has good development and application prospects. The application of Houttuynoid D in preparation of the medicine for treating prostatic cancer provided by the invention is disclosed firstly. The skeleton type belongs to new skeleton type, and the inhibitory activity of Houttuynoid D on prostatic cancer cells is unexpectedly strong.
WO2009153178A3 Aryl ketone as mri This invention pertains to aryl pyrrolidinyl and piperidinyl ketone compounds of formula (I) wherein R1 and R2 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, and methods for using the same. In particular, compounds of the present invention are useful for treatment of diseases associated with monoamine reuptake inhibition.
CN101955462A Fenticonazole nitrate, preparation of levorotatory form and dextrorotatory form and application of levorotatory form in preparing antifungal medicaments The invention relates to a synthesis process for fenticonazole nitrate. In the synthesis process, thiophenol and para aminobenzoic acid are taken as raw materials, and are subjected to seven-step reaction to form the fenticonazole nitrate, and the yield is higher. The invention relates to a preparation method for a levorotatory form and a dextrorotatory form of the fenticonazole nitrate, which solves the problem that the levorotatory form and the dextrorotatory form cannot be well obtained due to complicated and fussy operation according to documents. The levorotatory form and the dextrorotatory form have high purity and high industrial application value. Experiments prove that the antibacterial activity of the levorotatory form of the fenticonazole nitrate is greater than that of racemate and the dextrorotatory form. The invention relates to application of the levorotatory form of the fenticonazole nitrate in preparing antifungal medicaments.
US20120172423 Compositions and methods for treating herpes simplex virus Green tea polyphenol compositions and methods of their use in treating herpes simplex virus (HSV) are provided. Representative green tea polyphenols include, but are not limited to (−)-epigallocatechin-3-gallate as well as green tea polyphenols with one on more ester-linked fatty acids.
CN103704711A Granules with anti-fatigue and health-care function The invention discloses granules with an anti-fatigue and health-care function. The granules are prepared from following main components: 0.1g-5g of creatine, 1g-3g of calcium beta-hydroxy-beta-methyl butyrate, 1g-10g of fructose, 1g-500g of protein powder, 3g-9g of pseudo-ginsengs, 9g-30g of codonopsis pilosula, 10g-15g of radix puerariae, 9g-27g of acanthopanax senticosus, 6g-12g of American ginsengs and 0.1g-1.4g of taurine. The granules with the anti-fatigue and health-care function have the anti-fatigue and health-care function; the malnutrition is improved; the granules have an obvious effect to promote the recovery after exercises.
EP2740744A2 SP35 antibodies and uses thereof Endogenous Sp35 is a negative regulator for neuronal survival, axon regeneration, oligodendrocyte differentiation and myelination. Molecules that block endogenous Sp35 function, such as anti-Sp35 antibodies can be used as therapeutics for the treatment of neuron and oligodendrocyte dysfunction. The present disclosure provides antibodies specific for Sp35, and methods of using such antibodies as antagonists of endogenous Sp35 function. The disclosure further provides specific hybridoma and phage library-derived monoclonal antibodies, nucleic acids encoding these antibodies, and vectors and host cells comprising these antibodies. The disclosure further provides methods of promoting oligodendrocyte survival and myelination in a vertebrate, comprising administering to a vertebrate in need of such treatment an effective amount of an anti-Sp35 antibody.
WO2014017342A1 Indole derivative or pharmacologically acceptable salt thereof The present invention provides a compound represented by general formula (I), which has an EP1 receptor antagonist activity, or a pharmacologically acceptable salt thereof. The compound (I) of the present invention can be used as a therapeutic agent or prophylactic agent for LUTS, especially for various symptoms of OABs. (In the formula, A represents a pyridine ring or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; R1 represents a hydrogen atom or the like; R2 represents a C1-6 alkyl group; R3 represents a hydrogen atom or the like; R4 represents a hydrogen atom or the like; R5 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like; R6 represents a C1-6 alkyl group, a C3-6 cycloalkyl group or the like; R7 represents a hydrogen atom or the like; X represents a methylene group; and Q represents a single bond or the like.)
CN1813746A Intravenous administration formulation of levogatifloxacin and its preparing method The present invention provides venous administration preparation of levogatixacin, including infusion preparation, injection and freeze-dried powder injection. Its preparation method includes the following steps: (a), weighing levogatixacin and auxiliary material, adding partial injection water, stirring and dissolving; (b), using acid for venoclysis to regulate pH to 3.5-5.5, adding injection water to required quantity, adding injection active carbon, uniformly stirring them, standing still for 15 min, using titanium rod to remove carbon, utilizing microporous membrane to make fine filtration; (c), filling and sealing; and (d), freeze-drying to obtain freeze-dried preparation, sterilizing by using flowing steam or hot pressure so as to obtain injection.
CN102743388A Composition used for inhibiting bacteria generating novel beta lactamase The invention discloses a composition used for inhibiting bacteria generating novel beta lactamase. The composition is advantaged in that the active components of the composition comprise cefepime and tazobactam with a weight ratio of 2-6:1. According to the invention, the composition used for inhibiting the bacteria generating novel beta lactamase has a good inhibiting and/or killing effect against the bacteria generating novel CTX-M enzyme and AmpC enzyme, and is especially effective against bacteria with drug resistance to CTX-M enzyme and AmpC enzyme hydrolysis effects. The composition has good practicality, and provides good economic and social effects.
CN101314793A Method for detecting ovarian cancer and method for suppresssing the same The invention provides a method for detecting the ovarian cancer including the vicious degree through the change of the genome structure in the ovarian cancer as an index. The invention can detect the ovarian cancer including the vicious degree using the change of the genome structure in the ovarian cancer as an index. In addition, in the ovarian cancer, through recovering the deactivated gene, the multiplication of the ovarian cancer can be restrained.
CN103288721A (4-(4-[6-(trifluoromethyl-pyridin-3-ylamino)-n-containing-heteroaryl]-phenyl)-cyclohexyl)-acetic acid derivatives and pharmaceutical uses thereof The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
CN101849921A Extended release tablet formulation containing pramipexole or a pharmaceutically acceptable salt thereof The invention is directed to an extended release tablet formulation comprising pramipexole or a pharmaceutically acceptable salt thereof in a matrix comprising at least two water swelling polymers, wherein one polymer is pregelatinized starch, the other polymer is anionic polymer.
CN102060869A Tindiphenyl (IV) coordination compound of benzoylformic acid-3-hydroxyl-2-naphthyl formyl hydrazone as well as preparation method and application thereof The invention discloses a tindiphenyl (IV) coordination compound of benzoylformic acid-3-hydroxyl-2-naphthyl formyl hydrazone, which has a structural formula shown in the specification. The preparation method comprises the steps of: adding a mixture of benzoylformic acid-3-hydroxyl-2-naphthyl acyl hydrazone, diphenyl tin oxide, methylbenzene and ethanol into a reaction vessel, stirring for backflow for 6-7 hours at a temperature of 70 to 85 DEG C, cooling to room temperature, and rotationally evaporating to obtain an orange-yellow solid; then recrystallizing to obtain the tindiphenyl (IV) coordination compound of benzoylformic acid-3-hydroxyl-2-naphthyl formyl hydrazone. The coordination compound has higher anticancer activity and can be used as a raw material to prepare medicines for treating human liver cancer, human lung adenocarcinoma, human leukemia or human colon cancer. Compared with generally-used platinum-based anticancer medicines, the organic tin coordination compound has the characteristics of high anticancer activity, good lipid solubility, low cost, simple preparation method and the like and provides a new approach to the development of anticancer medicines.
CN1569902A Active oligose derivative and its preparation method The invention discloses active oligose derivative and its preparation method, wherein the exhibited activities include AIDS virus resistance, anticoagulant, and antineoplastic. The invention also provides the construction for the compound and process for preparation.
US7198790 Growth differentiation factor-5 Growth differentiation factor-5 (GDF-5) is disclosed along with its polynucleotide sequence and amino acid sequence. Also disclosed are diagnostic and therapeutic methods of using the GDF-5 polypeptide and polynucleotide sequences.
CN103304584A 2-hydrazone-thiazolo[4,5-b]quinoxaline compounds, and preparation method and purpose thereof The invention relates to 2-hydrazone-thiazolo[4,5-b]quinoxaline compounds which are characterized in that the compounds have a general formula represented as the following, wherein R is as the following. The 2-hydrazone-thiazolo[4,5-b]quinoxaline compounds provided by the invention can be used as potential antibacterial and antitumor medicines. The invention also discloses a preparation method thereof.
US7604812 For the treatment of dry, sensitive skin. Despite being free from such ingredients as perfumes, preservatives, colorings, plant extracts, PEGs, cetylstearyl alcohol, lanolin alcohol, lower alcohols and proteins The invention provides novel hypoallergenic and non-irritant medical skin care formulations being water-in-oil emulsions. The formulations are free from ingredients with a known allergenic potential, such as fragrances, preservatives, colorings, plant extracts, PEGs, cetylstearyl alcohol, lanolin alcohol, lower alcohols and proteins, thus being particularly suitable for patients with sensitive dry skin. The skin care formulations of the invention are useful in the prophylaxis and treatment of dry, sensitive skin or in the therapy or therapy support of eczematous or psoriatic skin and exhibit favorable sensorial properties. The invention furthermore provides a method of manufacturing the novel hypoallergenic and non-irritant skin care formulations.
CN101759708A Cefodizime sodium crystal form and preparation method thereof as well as drug compound comprising crystal form The invention provides a cefodizime sodium crystal form. In the X-ray diffraction pattern of the crystal form, a 2 theta angle is expressed to have peaks at the locations of 3.8 degrees and 6.8 degrees as well as 10.2 degrees and 21.7 degrees; the error is between plus or minus 0.2 degree; in a differential thermogram, an endothermic peak is located at 66-72 DEG C and an exothermic peak is located at 252-256 DEG C. The invention also provides a method for preparing the cefodizime sodium crystal form and a drug compound comprising the cefodizime sodium crystal form. The cefodizime sodium crystal form product of the invention is granulated and has good flowability, is not needed to be crushed when being applied to preparation, has small static electricity, and saves equipment, power and human resource costs for industrial production. The crystal form cannot be caked during drying, is easy to be operated, has low organic residue and meets relevant national standards.
US20090163565 Compounds with nootropic action, their preperation, pharmaceutical compositions containing them, and use thereof Described herein are new bicyclic arylimidazolones having nootropic action (i.e., protecting and stimulating cerebral functions), analgesic action and anti hyperalgesic action; also described is the process for their preparation and pharmaceutical compositions comprising them, useful for the treatment of cognitive deficits, and of various types of pain.
WO2010038241A2 Pharmaceutical compositions comprising of proton pump inhibitor, prokinetic agent and alginic acid Oral pharmaceutical compositions and process for preparing compositions comprising at least one gastric acid suppressing agent, at least one prokinetic agent and at least one alginic acid optionally with pharmaceutically acceptable excipients are provided; such that the gastric acid suppressing agent is present in a delayed release form, prokinetic agent is present in a bimodal release form such as an immediate release form, and a delayed release form to provide a dose with a lag time form and alginic acid is present in an immediate release form. The said compositions are useful in the treatment of gastric acid related disorders such as gastro esophageal reflux disease, reflux esophagitis, peptic ulcer, gastric ulcer, heartburn, sour stomach, acid ingestion, upset stomach and/or pain associated with heartburn, sour stomach and acid ingestion, bloating, fullness, dyspepsia, nocturnal heartburn, disorders not manifested by the presence of ulcerations in the gastric mucosa, including chronic active or atrophic gastritis, and Zollinger-Ellison syndrome.
CN101822777A Preparation of transdermal medicine infusion patch for preventing/curing swine flue and preparation method thereof The invention discloses a preparation of transdermal medicine infusion patch for preventing/curing swine flu and a preparation method thereof, relating to a medicament for preventing/curing swine flu and the preparation method thereof. The materials comprise golden thread, baical skullcap root, salivia chinensis, pinellia tuber, indigowoad leaf, heartleaf houttuynia herb, semen lepidii, sweet wormwood herb, sweet basil, forsythia suspensa vahl, agastache rugosus, ephedra herb, almond, caladium, stiff silkworm, cape jasmine fruit, rehmanniae praeparatum, liquoric root, anemarrhena and gypsum, and are make into the transdermal medicine infusion patch for preventing/curing swine flu by a special process. The preparation makes the medicine directly delivered to the human target tissue (focus), ensures obvious effect and no toxic and side effect and acts perfectly well in preventing and curing the acute respiratory infectious disease, and is safe, convenient and effective and applicable to prevention/curing of H1N1 influenza virus.
US7262211 Activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful for Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.
CA2375727C Cytofectin dimers and methods of use thereof A composition is provided comprising a novel cationic lipid compound having hydrophobic tails and two quaternary ammonium headgroups bridged by a linker. The composition is useful as a cytofectin for facilitating delivery and transfection of biologically active agents, particularly anionic bioactive agents such as DNA, into cells. The composition is useful also as an adjuvant for enhancing the humoral immune response of a vertebrate to an immunogen, especially an immunogen encoded by a polynucleotide-based vaccine. In certain preferred embodiments, the cationic lipid compound is a dimer containing quaternary ammonium headgroups bridged by a linker having DNA and/or cell receptor binding affinity, such as a polypeptide or polyamine. Also disclosed is an immunogenic composition comprising an immunogen and the composition of the present invention.
CN101759763A Triptolide derivative, and preparation method and application thereof The invention discloses triptolide derivative, and a preparation method and application thereof. The triptolide derivatives has the general formula as shown in Formula (I), wherein R is selected from chlorine, amine, fatty amine or aromatic amine. In the invention, triptolides, which are natural products in plants, are used as lead compounds to be modified in structure, thereby obtaining compounds capable of resisting chronic granulocytic leukemia activity in different degrees. The compounds have strong activity for inhibiting and resisting leukaemia cells, and have especially strong activity for inhibiting the chronic granulocytic leukemia cells resisting STI571. The invention lays foundation for the triptolide derivatives to develop into novel medicaments for treating the chronic granulocytic leukemia, can be used for preparing medicaments for treating the chronic granulocytic leukemia, and has good application prospects.
WO2007058805A3 Compositions and methods for treating cns disorders The invention generally relates to thienopyridinone 5-HT4 receptor modulators, and in particular the use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating Alzheimer's disease, cognition disorders, depression, and anxiety.
CN101579399A Pharmaceutical composition for reducing blood sugar and blood fat, and curing diabetes The invention relates to a pharmaceutical composition for reducing blood sugar and blood fat, and curing diabetes, comprising milk veteh, dogwood, vitamin A, beta-renieratene, vitamin B complex, vitamin C, vitamin D, vitamin E, macroelements of calcium and magnesium and trace elements of zinc, selenium, chromium, copper, molybdenum and manganese. The composition is mainly suitable for hyperglycemia, hyperlipemia and diabetes crowds, is curative for reducing blood sugar, blood fat and curing diabetes, and can be used for a long time or according to the course of treatment.
CA2272720C New butyric esters with antiproliferative activity and the pharmaceutical compositions containing them The present application describes total or partial butyric esters of polysaccharides as novel compounds; the number of hydroxyl groups esterified with butyric residues per each glycosidic monomer is preferably higher than 0.001; the application also describes the process of preparation of said esters, their use in therapy as antiproliferative agents, and pharmaceutical compositions containing them.
WO2012028543A1 Composition comprising a combination of dha and epa for administration prior to commencement of chemotherapy The invention relates to a composition comprising a combination of the omega-3 fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA). The composition can be used for enhancing the activity of chemotherapy or radiotherapy and/or in the prevention or reduction of side effects caused by the chemotherapy or radiotherapy in a patient ill with cancer, the composition being intended for administration to the patient prior to the commencement of a cycle of chemotherapy or radiotherapy.
US20120328705 Magnetic nanomedicine for tumor suppression and therapy A magnetic nanomedicine for tumor suppression and therapy, comprising: a core, made of magnetic nanoparticles; a shell, encapsulating said core and is made of carboxylated polyaniline (SPAnH); and a tumor suppression medicine Epirubicin (EPI) or Doxorubicin (DOX) covalently bonded onto said shell. Said magnetic nanomedicine is capable of improving its thermal stability, and it can be dissolved uniformly in water, plus its superparamagnetic property, thus it can be guided by an outside magnetic field to concentrate to the site of tumor distribution to increase the local medicine concentration and enhance therapy effect.
US20060084141 Biosynthetic gene cluster for the maytansinoid antitumor agent ansamitocin The present invention relates to compositions and methods involving antitumor agents derived from bacteria. In particular, the present invention provides the ansamitocin biosynthetic gene cluster for the production of novel maytansinoid analogs with potent antitumor activity and reduced human toxicity.
US20090191177 Enantiomerically Pure (-) 2-[1-(7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-A]pyrimidin-9-yl)ethylamino]benzoic Acid, Its Use In Medical Therapy, And A Pharmaceutical Composition Comprising It - 026 The present invention relates to enantiomerically pure (−) 2-[1-(7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)ethylamino]benzoic acid or pharmaceutically acceptable salts thereof, it being in a solid state, its use in medical therapy, pharmaceutical composition comprising it, its use in the preparation of a medicament for use in a method for preventing or treating diseases, and its use in method for preventing or treating disease. The present invention relates to a selective inhibitor of phosphoinositide (PI) 3-kinase β and use of the selective inhibitor in e.g. anti-thrombotic therapy.
CA2464333C Heteroindanes: a new class of potent cannabimimetic ligands One aspect of the invention is concerned with cannabimimetic heteroindane analogs having affinities and/or selectivities for a cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.
CA2242879C Method for treating sexual dysfunctions This invention is a novel treatment for sexual dysfunctions by administering to a subject exhibiting a sexual dysfunction compounds that upmodulate the AMPA receptor. Methods and compositions for treating sexual dysfunction are provided. Kits containing the compositions in appropriate form for administration are also provided.
WO2006034849A1 Antitumoral pharmaceutical compositions comprising a spisulosine and a cyclodextrin The present invention relates to a pharmaceutical composition, in particular to a composition comprising a spisulosine compound and a cyclodextrin or cyclodextrin derivative, and its use in the treatment of cancer. The pharmaceutical composition has long term stability upon storage and does not form gels or precipitates when diluted for administration for long periods of time.
US20050267136 Method of inhibiting dihydrofolate reductase; screening assay for the identification of novel therapeutics and their cellular targets A novel screening assay for identifying therapeutic agents and their cellular targets is described. The assay is useful in developing new antibacterial, antifungal, antiparasitic and anti cancer therapeutics. New inhibitors of dihydrofolate reductase (DHFR) have been identified and their cellular target confirmed using the assay of the present invention. Methods of treating diseases that benefit from an inhibition of DHFR are also described.
CN102078292A Collagen oral liquid with improved bioavailability The invention provides a collagen oral liquid with improved bioavailability, comprising bioabsorbable collagen and a stabilizer capable of promoting dispersion of the collagen. The collagen oral liquid provided by the invention contains higher content of the bioabsorbale collagen, wherein the molecular weight of the bioabsorbale collagen is from 2500D to 3500D and the content of the bioabsorbale collagen is no less than 10% (g/ml). The stabilizer capable of promoting dispersion of the collagen adopted by in the invention is selected from hydroxypropyl methyl cellulose (HPMC), sodium alginate, sodium carboxymethyl cellulose, methyl cellulose, xanthan gum and non-ionic surfactant, wherein the non-ionic surfactant contains aliphatic chains and the hydrophile-lipophile balance (HLB) value of the non-ionic surfactant is from 7 to 13. The collagen oral liquid provided in the invention is used to improve skin condition and prevent bone joint diseases.
CN101502588B Composition for beauty treatment and removing blain and method for preparing the same The invention discloses a composition for beautifying and eliminating acne and a preparation method thereof, and the composition for beautifying and eliminating acne is prepared by the following raw materials of dried rehmannia root, gypsum, loquat leaf, tree peony bark, cape jasmine fruit, red paeony root, baical skullcap root, white mulberry root-bark and liquoric root. The prepared compositionfor beautifying and eliminating acne can be prepared into any one commonly used formulation for oral administration, the efficacy for the acne is significant, the total effective rate can be more than 98 percent, and the composition can also lead skin to be delicate, white, tender and elastic.
US8202847 Mutant human CD80 and compositions for and methods of making and using the same Improved vaccines and methods of using the same are disclosed Immunosuppressive compositions for treating individuals who have autoimmune diseases or transplants and methods of using the same are disclosed.
CN101429218A Preparation of novel organic platinum complex and uses thereof The invention relates to preparation and application of a novel organo-antimony complex (1). The complex (1) has the characteristics of high anticancer activity, large water solubility, small toxic side effect and the like. A drug effect composition containing the complex (1) is used for treating various solid cancers, such as lung cancer, gastric carcinoma, liver cancer, breast carcinoma, cancer of colon, ovarian cancer, cervical carcinoma, leukemia, lymphoma, nasopharyngeal darcinoma and the like.
WO2013007700A1 Pharmaceutical composition comprising oleic acid, palmitic acid, linoleic acid and linolenic acid "Pharmaceutical composition". In a first aspect, the present invention relates to a topical cosmetic, dermatological or pharmaceutical composition comprising a mixture of acids consisting of 85-97% by weight of oleic acid, 1.5-6% by weight of palmitic acid, 1.5-6% by weight of linoleic acid, and 0.2-6% by weight of linolenic acid, with respect to the total weight of the acid mixture. In a preferred aspect, the composition of the present invention further comprises hydrogen peroxide. In a second aspect, the present invention relates to a method for preparing such cosmetic composition by mixing such acid mixture with hydrogen peroxide.
CN102872357A Medicine for oral administration for treating carbuncle, gastritis, gastric ulcer and early gastric cancer and method for preparing medicine for oral administration The invention relates to a medicine for oral administration for treating carbuncle, gastritis, gastric ulcer and early gastric cancer. The medicine for oral administration comprises, by weight, from 1 to 2 parts of bamboo skin, from 0 to 2.5 parts of cortex lycii radicis, from 1.5 to 2.5 parts of Chinese honeylocust leaves, from 1 to 3 parts of dandelion, from 20 to 60 parts of soybeans and from 0.6 to 2 parts of edible calcined gypsum. The invention further provides a method for preparing the medicine for oral administration. The medicine for oral administration has effects of replenishing and activating blood, expelling noxious substances, diminishing inflammation, relieving swelling and pain, promoting blood circulation to remove blood stasis, eliminating necrotic tissues, promoting granulation, healing sore and the like, has the outstanding advantages of capability of becoming effective fast, short treatment course and obvious curative effect, can be taken conveniently, and is free of toxic and side effects, raw materials of the medicine are cheap and are good in compatibility, sources of the raw materials are abundant, and the preparation process is easy to control, popularize and apply.
CN101810638A Preparation method of endogenous interferon inducer injection and nanometer microencapsulation solution The invention discloses a preparation method of endogenous interferon inducer injection and nanometer microencapsulation solution, relating to a pharmaceutical composition for treating and curing breeding animal viral infection by improving the inducement level of endogenous interferon. The invention uses endogenous interferon induction technology, avoids the defects of strong specificity of self species of interferon preparation, is convenient to apply in production and practice by drug administration in various modes and has the characteristics of low onset dose and the like, and degradation products can directly enter an animal body metabolic pool to continue metabolizing. In addition, the invention has an important meaning for effectively controlling raised animal viral infection and lowering drug residue harm.
EP2254574A1 Beta-lactones as antibacterial agents The present invention relates to specific beta-lactone compounds and compositions thereof for the treatment of infections, such as, e.g., infections with bacteria or infections with protozoa, in particular infections with Gram-positive and/or Gram-negative bacteria and of infectious diseases caused by or related to Gram-positive and/or Gram-negative bacteria, and to the modulation of virulence of Gram-positive and/or Gram-negative bacteria or of protozoa by specific beta-lactone compounds. The invention further relates to the use of the compounds or compositions for preventing or eliminating biofilms.
CA2759571A1 Two component interactive emulsion product The present invention describes the use of two oppositely charged surfactants as the primary emulsifiers in two separated parts of a product. The emulsifiers are chosen such that when the two parts of the emulsion product are mixed, the emulsifiers react to form water insoluble compounds that are no longer able to function as emulsifiers, thus, the oil phase of the emulsion is precipitated onto the skin along with the emulsifier reaction product. Since none of the deposited materials are water soluble, or capable of functioning as emulsifiers, the deposited oil phase is extremely resistant to being washed off. This technology finds applications in hand and body creams and lotions, baby care products, sunscreens, skin protective products, makeup systems, and automotive and furniture polishes.
WO2011150299A3 Treatment of myocardial infarction and vascular injury with netrin-1 Disclosed herein are methods for treating, inhibiting, or reducing ischemia/reperfusion injury of a cardiac tissue; increasing phosphorylation of ERK1/2 and/or eNOS in a cardiac tissue; treating, inhibiting, or reducing loss of NO; treating, inhibiting, or reducing uncoupling of NOS; increasing recoupling of NOS; treating, inhibiting, or reducing loss of DCC protein and mRNA expression in a cardiac tissue; decreasing or reducing the infarct size of a heart resulting from ischemia/reperfusion injury; decreasing or reducing superoxide production by a cardiac tissue caused by ischemia/reperfusion injury; treating, inhibiting, or reducing neointimal formation and restenosis; treating, inhibiting, or reducing apoptosis of mobilized endothelial progenitor cells; or a combination thereof of a blood vessel (such as an artery, a coronary artery, a vein, or a capillary) or a portion of the blood vessel in a subject which comprise the administration of netrin-1.
EP2303276A1 Fumarate salt of 4- (3-chloro-2-fluoroanilino) -7-methoxy-6- { [1- (n-methylcarbamoylmethyl) piperidin- 4-yl]oxy}quinazoline 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described.
EP2382213A1 One-step process for preparing paliperidone and its oxalate salt The present invention relates to a one-step process for the preparation of the antipsychotic agent Paliperidone by oxidation of Risperidone, and to Paliperidone oxalate or a hydrate, solvate or polymorph thereof.
EP1474415B1 1-phenyl-2-heteroaryl-substituted benzimidazole derivatives, the use thereof for producing drugs used in the treatment of immunological diseases The invention relates to the novel benzimidazole derivatives of formula (I), to the production and use thereof in the treatment and prophylaxis of diseases that are associated with microglial activation, and of T-cell mediated immunological diseases. The invention also relates to the pharmaceutical preparations that contain the novel benzimidazole derivatives.
EP1510208A1 Pharmaceutical composition comprising a combination of metformin and statin A pharmaceutical composition comprising: (i) metformin, optionally in the form of one of its pharmaceutically acceptable salts, (ii) a statin, optionally in the form one of its pharmaceutically acceptable salts, and optionally one or more pharmaceutically acceptable excipients, is suitable for use in the treatment of hyperglycemia non-insulin-dependent diabetes, dyslipidemia, hyperlipidemia, hypercholesterolemia, and obesity.
CN101384595B Salt of CD 80 antagonist The choline salt of the CD80 antagonist compound 4-(6-fluoro-3-oxo-1,3- dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-N-(2,2-difluoro-ethyl)-benzamide (I) has good aqueous solubility and is therefore convenient for pharmaceutical use.
WO2010016590A1 Therapeutic or prophylactic agent for generalized pain syndrome Generalized pain syndrome is a disease of which a causal factor has not been defined yet and for which a therapeutic method has not been established yet. Disclosed is a therapeutic or prophylactic agent for generalized pain syndrome. The therapeutic or prophylactic agent for generalized pain syndrome comprises an LPA1 antagonist or an autotaxin inhibitor as an active ingredient. The agent is preferably administered to the central nerve system. Generalized pain syndrome is preferably fibromyalgia, chronic fatigue syndrome or irritable bowel syndrome.
CN102002081A 9-O-beta-D-glucosyl nandinine as well as preparation method and application thereof The invention relates to the field of biological medicines, in particular to a 9-O-beta-D-glucosyl nandinine (I) and a preparation method thereof. The pharmacological test proves that the nandinine (I) of the invention has the efficacy of treating cardiovascular diseases.
CN101328166B 2-dihydroindole ketone derivate as protein kinase inhibitor and histone deacetylase inhibitor The invention discloses a method for preparing 3-(4-amide pyrrole-2- methylene)-2-indole ketone derivative and application thereof. The structure is shown as the formula (I), wherein the definitions of X, R<1>, R<2>, R<3>, R<4>, R<5> and n are stated in the instruction. The compound has the protein kinase inhibition activity and the histone sirtuin inhibition activity, and can be used for treating the diseases related to the abnormal protein kinase activity or the abnormal histone sirtuin activity such as inflammation, autoimmune diseases, cancer, nervous system diseases, neurodegenerative diseases, angiocardiopathy, hypersensitivity, asthma, and diseases related to hormone.
CN103694244A 3, 6 substituted-1, 2, 4-triazole [3, 4-alpha] phthalazine compound as well as preparation method and application of 3, 6 substituted-1, 2, 4-triazole [3, 4-alpha] phthalazine compound The invention belongs to the field of medicinal chemistry, and discloses a 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound having antitumor activity as well as a synthesizing method and application of the 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound. The 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound has a structure as shown in a general formula I, wherein R1 refers to H, methyl or phenyl; R2 refers to 4-fluorophenyl, 4-chloroanilino, 4-bromophenyl, 4-methoxyphenyl, 4-hydroxydiphenyl, 2-fluorophenyl, 3-trifluoromethyl)phenyl]amino, naphthylamine-1-yl, pyrrolidone-1-yl, piperidine-1-yl, 3,5-dimethyl piperidine-1-yl, morpholine-4-yl, or piperazidine-1-yl. The preliminary in-vitro antitumor activity finds that the serial compounds have obvious inhibit and killing effects on multiple tumor cells, and the 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound can act as an active ingredient to be applied to clinical prevention and cancer treatment after being developed into a novel medicament.
EP2692742A1 Novel preparation technique for higher-order structure that exhibits anti-cellular effect Disclosed is a novel means by which cyanoacrylate polymer particles still more useful as an antibacterial agent, an anticancer agent, etc., than conventional particles. The method for production of cyanoacrylate polymer particles according to the present invention comprises anionically polymerizing a cyanoacrylate monomer(s) in the presence of at least one selected from the group consisting of amino acids, amino acid derivatives, and oligomers and polymers thereof, and substantially in the absence of a saccharide and substantially in the absence of a polysorbate. Cyanoacrylate nanoparticles containing an amino-based molecule(s) exhibit their cell-damaging activity via specific adhesion to cells, and effectively inhibit the growth of cancer cells and bacteria. Their cell-damaging activity can be further increased by producing the nanoparticles by the above-mentioned novel production method.
CN102617679A Preparation method and application of connected conjugated linoleic acid and gemcitabine prodrug The invention relates to a preparation method and application of a connected conjugated linoleic acid and gemcitabine prodrug. The conjugated linoleic acid is connected with the gemcitabine via an amide bond. The preparation method comprises the following steps that: under the protection of nitrogen, the conjugated linoleic acid is dissolved in a solvent, and an activator is added at a low temperature of -15 DEG C under stirring to activate the conjugated linoleic acid to form a highly reactive mixed acid anhydride; the gemcitabine is dissolved in a solvent to be added dropwise to the mixed acid anhydride, and the reaction is undergone under stirring at room temperature; the solvent refers to one or a mixed solution of triethylamine, tetrahydrofuran, N,N-dimethyl formamide, and the activator is ethyl chloroformate; the reaction time is 2-72 hours, and the feed molar ratio of the gemcitabine to the conjugated linoleic acid is 1:(0.5-5); and the molar ratio of the activator to the conjugated linoleic acid is 1:(0.5-5). The object of the invention is to increase the anti-tumor efficacy of the gemcitabine.
EP1603580A1 Composition for administration of iron for the treatment of restless legs syndrome A method of treating Restless Leg Syndrome, includes administering to a subject an iron complex having an iron release rate greater than IDI. The iron release rate is determined at a concentration of at least 2,000 µg/dl.
WO2007143434A3 Indazole and isoindole derivatives as glucokinase activating agents Compounds are provided for use with hexokinases that comprise: Formula(I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
CA2283830C Composition for forming solid particles The composition for forming solid particles of the present invention comprises a biodegradable polymer, a solvent, a polyhydric alcohol, a viscosity-increasing agent, and an active drug, wherein the composition is in the form of an emulsion comprising a continuous phase rich in the polyhydric alcohol and the viscosity-increasing agent and a dispersed phase of liquid particles rich in the biodegradable polymer and the solvent, the dispersed phase being present in said continuous phase. The above composition can allow the carrier comprising an active drug to reach all corners of narrow periodontal pockets, and the carrier comprising the active drug has high retention in the periodontal pockets, whereby making it possible to maintain the active drug for a long period of time at a high concentration.
CN102532071A L-ascorbyl palmitate particles, and preparation method and application thereof The invention discloses L-ascorbyl palmitate particles with the particle size of 80-500mu m, and also discloses a preparation method thereof. The preparation method comprises the following steps of: (1) mixing L-ascorbyl palmitate powder and a solvent to ensure that one part of L-ascorbyl palmitate powder is dissolved in the solvent and the other part of L-ascorbyl palmitate powder exists in a solid form, and granulating to obtain wet particles containing L-ascorbyl palmitate; (2) drying the wet particles containing the L-ascorbyl palmitate obtained in the step (1); and (3) sieving the dried product in the step (2) to obtain the L-ascorbyl palmitate particles with the particle size of 80-500mu m. The invention also discloses application of the L-ascorbyl palmitate particles. By the technical scheme, the L-ascorbyl palmitate particles have high fluidity and dispersibility and small dust and are convenient to use.
EP2196201A2 Combination of an alpha-2-delta ligand with a pdev inhibitor or a muscarinic antagonist to treat lower urinary tract symptoms The invention relates to the use of a combination of an alpha-2-delta ligand with a compound selected from (i) a PDEV inhibitory compound; or (ii) a muscarinic antagonist; or pharmaceutically acceptable salts or solvates thereof, for the manufacture of a medicament for the treatment of LUTS associated with OAB and/or BPH.
US20100216841 4-Fluoro-Piperidine T-Type Calcium Channel Antagonists The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
CN101305000A 5-oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of C-FMS kinase The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula (I) or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein: W, A, Y, Z, R<101> and R<200> are described in the specification.
EP2558083A1 Methods for providing enhanced resveratrol activity using 4-acetoxy-resveratrol The present invention relates to a method of providing enhanced resveratrol activity comprising: administering a therapeutically effective amount of 4-acetoxy-resveratrol for the treatment of and preventing physiological and pathophysiological conditions mediated by (1 ) sirtuins, (2) estrogen and anti-estrogen hormone actions and (3) chemical interventions important for male and female health, aging, anti-aging and age-related disorders.
US20080242733 (-)-Pseudoephedrine as a sympathomimetic drug The present invention provides pharmaceutical compositions which include (−)-pseudoephedrine and a pharmaceutically acceptable carrier, wherein the (−)-pseudoephedrine is substantially-free of (+)-pseudoephedrine. In another embodiment, the present invention provides methods of relieving nasal and bronchial congestion and of inducing pupil dilation which include administering a pharmaceutically effective amount of (−)-pseudoephedrine to a mammal. The (−)-pseudoephedrine used in the present methods is substantially free of (+)-pseudoephedrine and also substantially free of side effects caused by administration of (+)-pseudoephedrine.
CN103446090A Application of Incarviatone A in liver fibroblast proliferation inhibiting drug The invention discloses application of Incarviatone A in preparation of a liver fibroblast proliferation inhibiting drug. A pharmacological test proves that the Incarviatone A can obviously inhabit occurrence and development of liver fibrosis and can be used for preparation of drugs for inhabiting liver fibrosis and preventing and curing liver cirrhosis. The application of the Incarviatone A in the preparation of the liver fibroblast proliferation inhibiting drug is disclosed for the first time. Due to the fact that the skeleton type is a novel skeleton type and the high liver fibroblast proliferation inhibiting activity of the Incarviatone A is previously unimagined, the possibility that other compounds give any revelation does not exist, and the Incarviatone A has outstanding substantive characteristics and meanwhile has a remarkable improvement in liver fibroblast proliferation inhibition obviously.
CN101991593A Application of quercetin in medicament preparation The invention discloses application of quercetin in medicament preparation. In the invention, the application in the preparation of medicaments and health products for treating cardiovascular diseases, medicaments and health products for treating cancer, antiviral medicaments, antibacterial medicaments, anti-inflammatory medicaments, medicaments for treating pulmonary fibrosis, medicaments and health products for treating diabetes as well as antioxidant medicaments and health products is included.
CN1823828A Medicine and frod dual purpose compound vitamin and compound microelement nutritive product for preventing and treating xeroma and its manufacturing method A nutrient used as both medicine and food for preventing and treating xerophthalmia is prepared from vitamins and trace elements. Its preparing process is also disclosed.
US20100160313 Discovery of novel anticancer compounds based on conformational sampling of quinoxalinhydrazide pharmacophore The present invention relates in general to anti-cancer drug design. More specifically, the invention provides methods of mapping and screening for anti-cancer agents using pharmacophore models. The invention demonstrates that, conformational sampling of a small lead molecule, followed by representative pharmacophore model development, is an efficient approach for rational design of novel anticancer agents with similar or better potency than the original lead but with different physicochemical properties.
WO2012015789A2 Composition and method for the topicaltreatment of dermatitis A composition for topical treatment of dermatitis is provided. The composition includes one or more anti-histamines or a pharmaceutically acceptable salt thereof; one or more polysaccharides; and one or more Group 1, 2, or 13 metal hydroxides. The dermatitis may be a poison ivy, poison oak, poison sumac, diaper rash, eczema, lichen simplex chronicus, rashes, dermatoses, seborrheic dermatitis, psoriasis, atopic dermatitis, or the combination thereof. A method of treatment of dermatitis is also provided.
CN101795682A Intravenous and oral dosing of a direct-acting and reversible P2Y12 inhibitor The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: (I) alone or in combination with a second agent which can be aspirin or a thrombolytic agent.
CN103735539A Use of coenzyme Q10 The invention discloses a coenzyme Q10, belonging to the field of a feed additive, and use of a coenzyme Q10 premix in preparation of a drug for preventing and treating podagra. The coenzyme Q10 premix comprises the following components by weight percent: 2-5% of coenzyme Q10, and 95-98% of a carrier. The coenzyme Q10 and the premix thereof disclosed by the invention have significant prevention and treatment effects on avian gout, the renal pathological damage caused by the avian gout of a laying hen can be significantly relieved, the poultry mortality rate is reduced, secondly, the coenzyme Q10 disclosed by the invention does not contain an organic ingredient, and is free of toxic and side effects on birds and beasts and free of toxicity on environment.
US20060078504 Sustanined-release pharmaceutical composition for lung administration The present invention provides a sustained-release pharmaceutical composition containing a pharmacologically active substance, the pharmaceutical composition being able to control the pulmonary absorption of the pharmacologically active substance and produce prolonged pharmacological effects when administered via the pulmonary route. The invention provides a pharmaceutical composition containing carrageenan and a pharmacologically active substance that can be administered via the lungs, a production method and use thereof.
EP1940807A1 Carbamoylbenzotriazole derivatives as inhibitors of lipases and phospholipases The invention relates to carbamoylbenzotriazole derivatives of general formula (I), which are defined as cited in the description, to their pharmaceutically applicable salts and to their use as medicaments.
US20080124329 Conditioned Cell Immunization The present invention provides methods and compositions for generating modulators capable of binding to antigens presented by a cell that has been exposed to cellular conditioning. The present invention also includes methods and compositions for the prevention, treatment and diagnosis of disorders using the antigen modulators. The present invention further provides methods for identifying novel molecular targets for the treatment of different disorders.
EP2438168A2 Polynucleotides for multivalent rna interference, compositions and methods of use thereof The present invention includes bivalent or multivalent nucleic acid molecules or complexes of nucleic acid molecules having two or more target-specific regions, in which the target-specific regions are complementary to a single target gene at more than one distinct nucleotide site, and/or in which the target regions are complementary to more than one target gene or target sequence. Also included are compositions comprising such nucleic acid molecules and methods of using the same for multivalent RNA interference and the treatment of a variety of diseases and infections.
US7125891 Such as (1-((2,3-dihydro-2-(4-propyl-1H-imidazol-2-yl)-1H-indol-1 -yl)carbonyl)propyl)-carbamate; for inactivation of cholecystokinins The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or —(CR4R5)m— wherein m is an integer 1 or 2; R4 and R5 are each independently from each other hydrogen or C1-4alkyl; R1 is C1-6alkylcarbonyl optionally substituted with hydroxy; C1-6alkyloxycarbonyl; aminoC1-6alkylcarbonyl wherein the C1-6alkyl group is optionally substituted with C3-6cycloalkyl; mono- and di(C1-4alkyl)aminoC1-6alkylcarbonyl; aminocarbonyl substituted with aryl; C1-6alkylcarbonyloxyC1-6alkylcarbonyl; C1-6alkyloxycarbonylaminoC1-6alkylcarbonyl wherein the amino group is optionally substituted with C1-4alkyl; an amino acid; C1-6alkyl substituted with amino; or arylcarbonyl; R2 is an optionally substituted 5-membered heterocycle, or R2 is optionally substituted benzimidazole; R3 is a bivalent radical —CH2CH2— optionally substituted with halo or phenylmethyl; or R3 is a bivalent radical of formula
CN101053588A Preparation method for compound arabinogalactan film coated tablets The invention discloses a producing method for compound arabinogalactan film-coated tablets (CAFT), which is characterized in that: having the arabinogalactan, astragalus root, fuling poris cocos as material to produce coated tablets. The arabinogalactan is extracted by Larix gmelinii Rupr. with a basic unit of its main chain 1,3-beta-D-galactose, and a side chain mainly composed of L-arabinose connecting to the main chain by 6-1. The primary chemical components of the astragalus root are astragaloside I, II, III, asragulus polysacharin A, B, C, D, flavone, alkaloid, glucuronic acid, and microelement Selenium and etc.; and the primary chemical components of the fuling poris cocos are beta-pachyman, pachymic acid, poriatin and beta-pachyman catabolic enzyme. Three medicines cooperate to improve the organism immune function.
DE102005035575A1 New heteroaryl derivatives are phosphodiesterase-4 enzyme inhibitors useful for the treatment of e.g. respiratory or gastrointestinal complaints or diseases, depression, Alzheimer's disease and Parkinson's disease Heteroaryl derivatives (1) and their racemates, enantiomers, diastereomers, acid addition salts, solvates, hydrates and deuterated forms are new. Heteroaryl derivatives of formula (1) and their racemates, enantiomers, diastereomers, acid addition salts, solvates, hydrates and deuterated forms are new. A : CO, C=NH, 1-6C alkylene or 3-8C cycloalkylene; B1>phenyl or an aromatic or non-aromatic ring optionally containing two or three heteroatoms of O, S or N and optionally substituted with OH, O-1-6C alkyl, O-1-6C-haloalkyl, halo, 1-6C alkyl or 1-6C haloalkyl; B2>phenyl or hetero aryl containing 2 or 3 heteroatoms of O, S or N; X : e.g. O or S; n : 0-3; either R1>e.g. H, 1-6C alkyl, 1-6C haloalkyl; and R2>H, 1-6C alkyl or 1-6C haloalkyl; or NR1>R2>non-aromatic heterocycle containing 2 or 3 heteroatoms of O or N; or R2>+N+A+B1>bicyclic group of formula (g); A : CO, C=NH or 1-3C alkyl; m : 1-3; B1>sulfonyl compound of formula (h); Z1>H, OH, halo, 1-6C alkyl, 1-6C alkanol, O(1-6C alkyl), 6-10C aryl, O-6-10C aryl, NH2, NH(1-6C alkyl), N(1-6C) alkyl or 3-7C cycloalkyl; and R4>e.g. 1-6C alkyl, 3-8C cycloalkyl, 1-6C haloalkyl, CN or halo. Full definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) a medicament combination comprising (1) and further active substance, such as beta-mimetic, anticholinergic, corticosteroid, further phosphodiesterase-4-inhibitors, leukotriene D4 antagonists, epidermal growth factor receptor inhibitor, dopamine agonists, H1-antihistaminic, platelet-activating factor antagonist and/or phosphatidylinositol-3 kinase inhibitor; and (2) intermediate compounds of formula (i-iii) or (I-V). PG : H or a suitable protection group; and G : NO2 or NH2. [Image] [Image] [Image] [Image] [Image] - ACTIVITY : Gastrointestinal-Gen.; Antidepressant; Neuroleptic; Antimanic; Neuroprotective; Nootropic; Antiparkinsonian; Analgesic; Cerebroprotective; CNS-Gen.; Respiratory-Gen.; Antiasthmatic; Antiinflammatory; Antiulcer. - MECHANISM OF ACTION : Phosphodiesterase-4 enzyme inhibitor.
CA2831143A1 Cyclopropylamines as lsd1 inhibitors This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1(LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
US20130034540 Immune Gene Signatures in Cancer This invention relates to methods for selecting a treatment, treating, and predicting survival time in subjects with cancer, such as colorectal cancer, based on tumor expression levels of chemokines, cytotoxic genes, and/or dendritic cell genes.
CN103328473A Substituted azaindazole compounds Disclosed are azaindazole compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein: Q is: (i) 5-membered heteroaryl comprising at least one nitrogen heteroatom and substituted with zero to 2 Rg; or (ii) 9- to 10-membered bicyclic heteroaryl selected from Formula (II) and; wherein Ring A is a 5- to 6-membered aryl or heteroaryl fused ring substituted with zero to 2 Rg; and R1, R2, R3, and Rg are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
CN101062925B Paclitaxel derivatives, preparation method and medicinal composition and usage thereof The invention discloses a new Paclitaxel derivant with second class amido group in lateral chain and good water-solubility as general formula (I), preparing method, medicinal compound with this chemical compound and application to prepare the cancer treatment medicine.
WO2010032461A1 Nitrogen-containing fused ring compound Disclosed is an acid secretion inhibitor containing a compound represented by formula (I), a salt thereof, or a prodrug of the compound or salt. (In the formula, R1's may be the same or different and each represents a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted alkoxy group, a hydroxy group or an optionally substituted amino group; R2 represents a hydrogen atom or a substituent; R3 represents a hydrogen atom or a substituent; ring A represents an optionally substituted carbon ring or an optionally substituted heterocyclic ring; and n represents an integer of 1-4.)
CN101537010B Eyedrop preparation and preparation method thereof The invention discloses a doxycycline eyedrop preparation and a preparation method thereof. The doxycycline eyedrop preparation comprises 0.03 to 0.5 wt percent of doxycycline, distilled water, hydroxypropyl-beta-cyclodextrin and an antioxidant and has a pH value of 5.0 to 6.0, wherein the weight ratio of doxycycline to hydroxypropyl-beta-cyclodextrin is 1: (1 to 50). The doxycycline eyedrop preparation can improve the dissolubility, the dissolving rate and the stability of doxycycline medicines.
CA2168584C A method for sensitization of cancer cells for killer cell mediated lysis The invention relates to a method of sensitizing cancer cells for a killer cell mediated lysis which involves administering to a patient an effective amount of antiestrogen and killer cells either jointly or sequentially, wherein the killer cells are selected from the group of NK cells, LAK cells and CTL cells and the antiestrogen is selected from the group of triphenylethylene class antiestrogens, such as tamoxifen or toremifene or their pharmaceutically acceptable salt.
US20080317834 Compounds and methods for modulating cerebral amyloid angiopathy The invention provides methods of inhibiting cerebral amyloid angiopathy. The invention further provides methods of treating a disease state characterized by cerebral amyloid angiopathy in a subject.
CN1917883B Use of treprostinil in preparing medicine to improve kidney functions The present invention describes novel methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for improving kidney functions, such as urine output, and treating symptoms associated with kidney malfunction or failure. The invention also relates to kits for the improvement of kidney functions and the treatment of symptoms associated with kidney malfunction or failure, comprising an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.
CN103622906A High drug-loading capacity amphotericin B polymer composite micelle and preparation method thereof The invention belongs to the field of biotechnology and particularly relates to a high drug-loading capacity amphotericin B polymer composite micelle and a preparation method thereof. According to the invention, polyethylene glycol-phospholipid with clinical application potentials and indissolvable amphotericin B are used to form amphotericin B polyethylene glycol-phospholipid composite micelle; amphotericin B can combine with polyethylene glycol-phospholipid to form the amphotericin B polymer composite micelle with high drug-loading capacity, high encapsulation efficiency and high stability through the electrostatic attraction function and the interaction between carbon chains. The amphotericin B polymer composite micelle is stable in normal saline and plasma and lower in toxicity and infusion reaction, can be diluted by adopting normal saline, and greatly improves the clinical application range and convenience.
WO2010139731A1 1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c] quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H- imidazo[4,5-c] quinofinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c] quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1 H- imidazo[4,5-c] quinolinone derivatives; and a process for the preparation of the novel 1H- imidazo[4,5-c] quinolinone derivatives.
CN101953840A Compound vitamin composition for injection and preparation method thereof The invention relates to a compound vitamin composition for injection, which comprises water-soluble vitamins and liposoluble vitamins including but not limited to group B vitamins, vitamin C, vitamins A, D, E and K, and pharmaceutically acceptable auxiliary materials. The preparation method comprises the following steps of: taking the various vitamins as raw materials according to the technical method, adding auxiliary materials in specific varieties and ratios, and developing into a nutritional preparation for intravenous supply. The compound vitamin composition for injection can be used for maintaining patient nutrition.
WO2007034445A3 Novel piperazine derivatives as renin inhibitors for cardiovascular events and renal insufficiency The invention relates to novel piperazine derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin. In particular, the present invention relates to novel compounds of the formula (I),
WO2007057763A2 Nitric oxide as an anti-viral agent, vaccine and vaccine adjuvant The invention relates to uses of nitric oxide gas to inactivate any whole, part or subunit of a microbe, such as a virus. Such an inactivated or attenuated virus after treatment with NO gas may be used in formulations for a vaccine. Nitric oxide may be administered directly to create a vaccine through in vitro and/or in situ or by direct administration in vivo. Also provided are methods for treating patients with viral infections through the inhalation of nitric oxide gas.
CN1899299A Chitosan powder medicine for fishing and its producing process The chitosan medicine powder for fish consists of chitosan of molecular weight smaller than 60 kD in 3-15 wt% and soluble starch. The preparation process of the chitosan medicine powder for fish includes the following steps: 1. treating chitosan with Co-60 source to irradiate chitosan in controlled irradiation condition to obtain chitosan in the required molecular weight; 2. weighing chitosan and starch; 3. mixing; and 4. packing and inspection. The chitosan medicine powder for fish has no drug resistance, small dosage for curing bacterial diseases and no medicine residue.
US20110086805 In vitro method for diagnosing skin cancer The present invention relates to an in vitro method for identifying an individual suffering from or having a predisposition to skin cancer, characterized in that it comprises the step of analysing a biological sample originating from said individual by a) detecting a polymorphism of the MATP/SLC45A2 gene (SEQ ID NO: 1), and/or analysing the expression of the MATP/SLC45A2 gene; to the use, for preparing a composition for the treatment and/or prevention of a skin cancer in an individual, of a compound which specifically increases the expression of the MATP/SLC45A2 gene in a skin cell; and to a method for the selection, in vitro, of a compound capable of being of use in the treatment of skin cancer.
WO2008127678A1 Pyrido [2, 3-d] pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer The invention is directed to a Compound of Formula I, II, or III. The invention provides compounds that inhibit, regulate, and/or modulate PI3K that are useful in the treatment of hyperproliferatives diseases, such as cancer.
US7384975 Substituted furochromenes, preparation thereof and their antiinflammatory action The invention relates to novel compounds of the formula (I) including all their tautomers, to pharmaceutically acceptable salts and solvates thereof, to processes and reactive intermediates for the preparation thereof, and to processes and reactive intermediates for the preparation of the compounds of the formula (II) including all their stereoisomers and tautomers to the use of the compounds of the formula (II) as suitable precursors for the preparation of the compounds of the formula (I) as well as to use of the compounds of the formula (I) and of the compounds of the formula (II) as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diesases and conditions in humans.
CN1827585A Non-crystalline memantine hydrochloride The invention relates to a new type of 1-amido-3, 5-dimethyl tricyclic [3, 3, 1, 13, 7] decane hydrochlorate without crystalline phase, a preparing method and its medicinal agent. The material gained by this method is a useful medicine for curing dementia diseases such as Alzheimer's disease and diseases in relation to receptor antagonist of N- methyl-D- aspartate.
WO2011131661A1 1-(2-fluorobiphenyl-4-yl)-alkyl carboxylic acid derivatives for the therapy of transthyretin amyloidosis The invention relates to the use of derivatives of 1-(2-fluorobiphenyl-4- yl)-alkyl carboxylic acid as agents capable of stabilising the tetrameric native state of transthyretin for the prophylaxis and treatment of amyloidosis.
CN102861015A Stable amoxicillin and clavulanate potassium sustained release preparation and preparation technology The invention provides a stable amoxicillin and clavulanate potassium sustained release preparation, which is composed of a rapid-release layer and a slow-release layer. The weight ratio of amoxicillin to clavulanate potassium is 1000:62.5, the proportion of amoxicillin in the rapid-release layer and the slow-release layer is 1:1, all of clavulanate potassium is placed in the rapid-release layer, wherein the pharmaceutic auxiliary material comprises the following ingredients by weight: the ratio of amoxicillin to slow release material to lubricant to adhesive in the slow release layer is 500:140-150:5-10:16:23, the ratio of amoxicillin to clavulanate potassium to disintegrating agent to lubricant to coating powder in the rapid-release layer is 62.5:30-60:6-10:40-80. The amoxicillin and clavulanate potassium sustained release preparation has the characteristics of good stability, high curative effect, low side-effect incidence rate and reduced drug usage frequency.
US20110206781 Method to modulate hematopoietic stem cell growth Described herein are methods, compositions and kits related to manipulating hematopoietic stem cells (HSC) and more particularly to methods, compositions and kits related to increasing the number of hematopoietic stem cells in vitro, ex vivo and/or in vivo. Also described are methods, compositions and kits related to making an expanded population of HSC and methods, compositions and kits related to using the expanded population of HSC. For example, HSC growth may be enhanced by contacting the nascent stem cells or HSC with an agent that stimulates the nitric oxide signaling pathway.
CN103202882A Weight losing method for quickly decomposing fat and navel patch The invention discloses a weight losing method for quickly decomposing fat. The method is characterized by comprising the following steps of: during weight losing, drinking a cup of aqueous solution of vitamin B serving as an active ingredient with the effect of metabolizing the fat and lacking in body; after the solution of the vitamin B is drunk, taking exercise with a simulated biological motion instrument for 30 to 45 minutes to produce the metabolic cycle bionic effect so as to repair cells, decompose the fat and expel toxin; and sticking a navel patch to the navel for 10 to 18 hours so as to effectively limit the absorption of fat in food, accelerate the metabolism of the decomposed and semi-decomposed fat and control the diseases, wherein the navel patch is used once to twice every day, and ten days constitute a treatment course. The method has the advantages that the requirements of World Health Organization are met, three meals are eaten as usual, diarrhea, weakness and rebound are avoided, the method is scientific, reasonable and safe, the weight losing effect is good and the like.
WO2012147171A1 Biological function reviving agent The objective of the present invention is, by means of sodium hypochlorite, to heighten a biological function that plants and animals (including humans) are innately endowed with, to increase crop production, and to improve health and treatment resulting from regenerating aged or degraded tissues or organs of plants and animals (including humans). A further objective is to increase the function of chloroplasts in crops and to increase the regenerative power of aged or degraded tissues or organs of plants and animals (including humans). The objectives are achieved by means of: a biological function reviving agent that has sodium hypochlorite as the active ingredient; a plant activation method having a step for causing the seeds of a plant to absorb the reviving agent, sowing the seeds, and then raising the plants; and seeds that have absorbed the reviving agent.
CN102802638A Glycosaminoglycan mixtures The present invention relates to osteoblast derived glycosaminoglycan mixtures and to their use in one or more of: inhibition of osteoclastogenesis, enhancement of proliferation of osteoblasts, and/or the treatment or prevention of bone fracture or bone deterioration.
US20080020055 Phenylephrine Pharmaceutical Formulations and Compositions for Colonic Absorption The invention discloses a pharmaceutical composition comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is for oral administration wherein the composition delivers phenylephrine or a pharmaceutically acceptable salt thereof via absorption in the colon. The pharmaceutical composition comprises a core comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is in a time-dependent, pH-dependent, or colon-specific enzyme-dependent erodible layer that degrades to expose the core to release phenylephrine in the colon. In one preferred embodiment, the erodible layer encases the core. The composition optionally further comprises phenylephrine in the erodible layer or other additional layer(s). The pharmaceutical composition can further comprise one or more additional therapeutically active agents selected from one or more of the group consisting of antihistamines, analgesics, anti-pyretics, and non-steroidal anti-inflammatory agents. The invention also discloses methods of administering phenylephrine via the colon, thereby increasing the bioavailable amount of therapeutically active unconjugated phenylephrine relative to the total phenylephrine in the plasma.
WO2009026817A1 Compounds and composition used for inhibitting pge2 released from cmec 2-methoxy cinnamaldehyde, 2-methoxy cinnamyl alcohol, 2-methoxy cinnamic acid, cinnamaldehyde, cinnamyl alcohol, cinnamic acid and the composition containing said compounds are disclosed. They are used to prepare the medicine for inhibiting PGE2 released from CMEC in mammal, including human. They are also used to prepare the medicine for antipyretic.
US20090123422 Method of treating idiopathic pulmonary fibrosis with aerosolized IFN-y A method of treating idiophathic pulmonary fibrosis (IPF), comprising administering aerosolized interferon-γ in a therapeutically effective amount to achieve improved or ameliorated symptoms of IPF.
WO2008093064A1 L-ALANINE DERIVATIVES AS α5 BETA 1 ANTAGONISTS The present invention relates to formula (I) compounds that inhibit of a5b1 function, processes; for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.
US20120157460 Tetrahydro-azacarboline mch-1 antagonists, methods of making, and uses thereof The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
EP2508179A1 Use of L-Carnitine, salts and derivatives thereof for reducing or preventing fatigue and improving cognitive function The invention relates to the use of L-carnitine, a salt of L-carnitine, a derivative of L-carnitine and/or salt of a derivative of L-carnitine, as well as respective methods and compositions, for reducing or preventing fatigue and/or for improving cognitive function in an animal. The animal is preferably a healthy individual and the use is preferably a non-therapeutic use.
CN1861075A Injection use medicine composition contg. water-soluble 17-allylamino-17-demethoxy geldanamycin An injection of water-soluble 17-allylamino-17-demethoxy geldanamycin (17-AAG) for treating multiple kinds of cancers is prepared from 17-AAG and polyethanediol for increasing the solubility of 17-AAG in water.
WO2002102129A3 Process for the preparation of programmed liberation compositions with venlafaxine and the resulting product Process for the preparation of programmed liberation compositions with venlafaxinee and the resulting product, from which the resulting product allows a better absorption of the active principle and a drastic decrease of the adverse effects, due to the preparation methodology. The formulation comprises a first phase, in which the non-active cores are elaborated as spherical micro granules, from sugar and starch. In the second phase, it is added to them the active drug, as impalpable powder, utilizing as binding, a povidone alcoholic solution. In the third phase, it is applied the coating on the micro granules that contain the active drug. At last, in the fourth phase, it is made the encapsulation of the recoated micro granule.
WO2014163512A1 Therapeutic compositions comprising extracts of propolis and uses thereof This invention provides pharmaceutical compositions comprising compounds including 5-phenylpenta-2, 4-dienoic acid, 3-methyl-3-butenyl caffeic acid, 1,1-dimethylallyl caffeic acid, pinobanksin-3-acetate, tectochrysin, pinostrobin chalcone, benzyl ferulate and benzyl isoferulate. Methods of using such compositions, in particular in the treatment or prevention of gastrointestinal cancers, and the resensitisation of gastrointestinal cancers to therapy are also provided.
WO2006101434A1 NOVEL TETRAHYDRO-1H-PYRIDO [4,3-b] INDOLE DERIVATIVES AS CB1’ RECEPTOR LIGANDS Compounds of Formulae I, or pharmaceutically acceptable salts thereof: wherein R1, R2 and R3 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
CN101530394B Preparation method of polypeptide-chitosan composite nanoparticles loaded with coenzyme Q10 The invention relates to coenzyme Q10 loaded polypeptide-chitosan composite nanoparticles and a preparation method thereof. The method comprises that: poly-L-glutamate-gamma-benzyl-polyethyleneglycol segmented copolymer and the coenzyme Q10 are mixed at room temperature, and are dissolved in mixed solvent of dimethyl formamide and tetrahydrofuran; after dialysis, centrifugalization and the like, supernatant liquor is filtered to obtain a coenzyme Q10-polypeptide drug-loaded micelle solution, and acetic acid is added to regulate pH value; meanwhile, chitosan is dissolved in the acetic acid solution with the same pH value, and is mixed with the coenzyme Q10-polypeptide acetic acid, and trimeric sodium phosphate solution is dripped in the mixture, thereby obtaining the coenzyme Q10 loaded polypeptide-chitosan composite nanoparticles with particle diameter of between 80 and 900nm, average drug-loaded ratio of between 2 to 20 percent, and envelop rate of between 30 and 70 percent. The nanoparticles are coenzyme Q10 nanometer hydrophobic drug particles with higher stability, slow release, and good biocompatibility.
CN101269055A Ambroxol hydrochloride oral cavity disintegrating tablet and method of producing the same The invention discloses a drug compound and the preparation method thereof. The drug compound contains ambroxol hydrochloride as well as pharmacy-accepted filling agents, disintegrants, gkidants, lubricants and taste-rectifying agents, the single-dose form of which is an orally-disintegrated tablet. The drug compound has the potency of reducing the viscosity of sputum and eliminating phlegm.
US20070117860 Bicyclic indolinesulphonamide derivatives The invention relates to novel bicyclic indoline sulfonamide derivatives of general formula (I), methods for the production thereof, and the use thereof in medicaments, especially as potent PPAR delta agonists for preventing and/or treating cardiovascular diseases, particularly dyslipidemia, arteriosclerosis, and coronary heart diseases.
EP1377294B1 Use of neuroactive substances for the treatment of parkinsons disease and pharmaceutical combination The invention relates to a use of a first substance which at least partly blocks specific receptors for a given neurotransmitter post-synaptically and a second substance which initiates or promotes a deafferentation of the innervation related to the neurotransmitter, for the treatment of Parkinsons disease, the production of a pharmaceutical for the treatment of Parkinsons disease, or a pharmaceutical combination for the treatment of Parkinsons disease. The invention further relates to a pharmaceutical combination.
US20120100229 Treatment and Prevention of White Matter Injury with KATP Channel Activators The present invention includes a method of treating or preventing a CNS white matter injury in a patient in need thereof. The invention also includes a method of stimulating proliferation of a CNS cell in a patient in need thereof.
US20090270504 Treatment of Huntington's Disease With EPA Analysis of the huntington gene provides a method for identifying patients likely to respond to treatment of Huntington's disease with eicosapentaenoic acid, EPA.
EP1951234A2 Method of inhibiting flt3 kinase A method of reducing or inhibiting kinase activity of FLT3 in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 using a compound of the present invention (I), or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
EP1218004B1 5-methyl indirubin for use in the treatment of human solid tumors The present invention relates to the use of cell membrane penetrating indigoid bisindole derivatives for the manufacture of a medicament for the treatment of human solid cancers.
WO2014142086A1 Pyrrolidin-3-yl acetate derivative and piperidin-3-yl acetate derivative In the present invention, a pyrrolidin-3-yl acetate derivative or piperidin-3-yl acetate derivative, or a pharmacologically acceptable salt thereof, has an inhibiting effect in the fractalkine-CX3CR1 pathway.
US7071222 Preparation containing a combination of 5-methylisoxazole-4-carboxylic acid-(4-trifluoromethyl)-anilide and N-(4-trifluoromethylphenyl)2-cyano-3-hydroxycrotonic acid amide A solid composition comprising 5-methyl-4′-trifluoromethyl-4-isoxazole carboxanilide and N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonic acid amide, suitable for treatment of immunological and cancerous diseases.
US20110015199 GPR119 Agonists GPR119 agonist compounds of the formula: and pharmaceutical compositions for the treatment of diabetes and obesity.
CN101574506B Method for preparing pingxiao preparation The invention relates to a method for preparing a pingxiao preparation of a prior Chinese patent drug, comprising the following steps: extracting radix curcumae naphtha, after the processes of diacolation, decoction and combination infusion and diacolation collation, decompressing and condensing to a thick paste, grinding into powder after drying at low temperature, then adding the fine powders ofnux vomica, dried lacquer, trogopterus, white vitriol, saltpeter as well as proper amount of auxiliary materials, mixing the above materials and adding diacolation collation, palletizing, drying at low temperature and adding naphtha, and mixing evenly to prepare various dosage forms. The invention has reasonable process, greatly improves the content of active ingredients of monarch drug in the pingxiao preparation, and improves the curing effect of pingxiao preparation of the prior Chinese patent drug.
EP1297828B1 Oral formulations for localized colonic release and the method of preparation thereof The present invention relates to oral formulations for localized colonic release, comprising metal salt of pectin, such as calcium pectinate with 5-12% of metal content, an pharmaceutically acceptable carriers or excipients. Said formulations may be the form of capsule or tablet. The methods for preparing said capsule and its shell with calcium pectinate are also disclosed.
US20120107421 Estrogen receptor alleles that are predictive of increased susceptibility to bone fracture In one aspect, the present invention provides methods of determining susceptibility to bone fracture in a mammalian subject, wherein the methods comprise analyzing nucleic acid molecules obtained from the mammalian subject to determine which of the P, p X, and x alleles of the estrogen receptor α gene are present, wherein the presence of a haplotype comprising the p and x alleles is indicative of an increased susceptibility to bone fracture. The present invention also provides kits for determining susceptibility to bone fracture in a mammalian subject.
CN103450174A Benzopyrone-phenyl-oxazolidone compounds as well as preparation methods and applications thereof The invention discloses benzopyrone-phenyl-oxazolidone compounds with the following structural general formulas as shown in the specification. The compounds have better inhibiting and killing effects on various germs, and some of the benzopyrone-phenyl-oxazolidone compounds have higher bacteriostatic activity than positive control penicillihe G, kalamycin and ketoconazole, so that the benzopyrone-phenyl-oxazolidone compounds can be used for preparing anti-infective drugs. The invention also discloses preparation methods of the benzopyrone-phenyl-oxazolidone compounds.
US20100003302 Vascular restenosis preventing agent and implantable intravascular device coated therewith A drug for preventing vascular restenosis comprises a compound that inactivates α1-protease inhibitor and α2-macroglobulin as active constituents, which are associated with occurrence of vascular restenosis after coronary artery intervention. Preferably, the drug is coated on a surface of an implantable intravascular device and locally administered to the affected area by application of the implantable intravascular device to a narrowed area.
US20120329813 Pemirolast for the Treatment of Systemic Low Grade Inflammation According to the invention there is provided pemirolast, or a pharmaceutically acceptable salt thereof, for use in the treatment of systemic low-grade inflammation.
CN1820736A Use of 1,4-naphthalene diphenol in preparing external use sperm killing contraceptive medicine of preventing and curing genital tract infection The present invention discloses the use of 1, 4-naphthalene diphenol in preparing external use spermicidal contraceptive capable of preventing and treating genital tract infection and the external use spermicidal contraceptive prepared with 1, 4-naphthalene diphenol. The external use spermicidal contraceptive possesses triple functions of diminishing inflammation, birth control and improving sexual life. The spermicidal contraceptive has powerful spermicidal effect 25 times higher than that of nonoxynol nonylphenoxy-polyethoxyethanol, no bacteriostasis on normal lactobacillus inside vagina and effect of defending partial STD pathogens. It has the features of safety, high efficiency and convenience.
US20110039888 Asymmetric alpha functionalization and alpha, alpha bisfunctionalization of aldehydes and ketones The present invention relates, generally, to asymmetric α-functionalization and to asymmetric α,α-bisfunctionalization of ketones and aldehydes and, in particular, to chiral auxiliaries suitable for use in effecting such functionalizations and to methods of using same.
EP1736149A2 Astaxanthin-containing agent for lowering neutral fat concentration in blood An agent for lowering neutral fat concentration in blood and a therapeutic agent for a disease to which neutral fat in blood is related, the agent containing astaxanthin and/or esters thereof . The agent for lowering neutral fat concentration in blood according to the present invention is useful for treating various diseases having an apparent relation to neutral fat in blood, such as arteriosclerosis, a cardiovascular disease, a cerebrovascular disorder, hyperlipemia, or a metabolic disorder.
EP2266985A1 Tricyclic Pyrimidine Derivatives as Wnt antagonists The present invention relates to compounds having the general formula (I) with the definitions of X1 - X3, Y1, Y2, L1, R1 and R2 given below and/or solvates, hydrates, esters and pharmaceutically acceptable salts thereof. Furthermore, the invention relates to the use of said compounds for modulating of the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.
US20080103105 Nervous system, neurodegenerative, and psychological disorders are treated using synergistic mixture of neurogenic agents; atorvastatin, cerivastatin, fluvastatin, simvastatin, lovastatin, pravastatin, rosuvastatin, or crilvastatin; and buspirone, ribavirin, tacrine, azakenpaullone, or folic acid The instant disclosure describes methods of treating diseases and conditions of the central and peripheral nervous system including by stimulating or increasing neurogenesis, neuroproliferation, and/or neurodifferentiation. The disclosure includes compositions and methods based on use of an HMGCR modulating agent, optionally in combination with one or more other neurogenic agents, to stimulate or increase a neurogenic response and/or to treat disease.
US20110077293 GAMBOGIC AMINE, A SELECTIVE TrkA AGONIST WITH NEUROPROTECTIVE ACTIVITY Small molecule agonists, partial agonists, and antagonists for the TrkA receptor are described. The compounds are gambogic amines, where the carboxylic acid group of gambogic acid (CO2H) has been replaced by an amine group (CH2NR1R2). In some embodiments, the compounds selectively bind to TrkA but not TrkB or C, robustly induce its tyrosine phosphorylation and downstream signaling activation including Akt and MAP kinases. Further, they can strongly prevent glutamate-induced neuronal cell death and provoke prominent neurite outgrowth in PC12 cells. Gambogic amines specifically interact with the cytoplasmic juxtamembrane domain of TrkA receptor and trigger its dimerization. Administration of these compounds in can substantially diminishes Kainic acid-triggered neuronal cell death and decrease infarct volume in transient middle cerebral artery occlusion (MCAO) model of stroke. Thus, these compounds can provide effective treatments for debilitating neurodegenerative diseases and provide neuroprotection from patients suffering from stroke or other ischemic events.
WO2013024495A1 Pharmaceutical formulations of cabazitaxel Aspects of the present application relate to pharmaceutical formulations comprising cabazitaxel or its pharmaceutically acceptable salts, isomers, racemates, enantiomers, hydrates, solvates, metabolites, polymorphs, and mixtures thereof. In embodiments, formulations are in the form of ready-to-use solutions or concentrates, or lyophilized forms. Further aspects relate to stable injectable compositions of cabazitaxel ready for direct dilution with infusion solution, without any need for preparation of premix solutions, and manufacturing processes thereof.
CN101181626B Transfer factor capsule and preparation method thereof The invention relates to a transferring factor capsule and the production method and belongs to the biological pharmacy technical field. The invention solves the technical problems that the produced capsule dosage is not accurate and the stability is poor, which is caused by the poor fluidity and much stronger humidity inducting capacity of the solid semi-finished product of the transferring factor during the production process of the capsule of the prior art. The transferring factor capsule of the invention is produced by the following materials by weight: 5.94 to 8.58 parts of transferring factor being counted as the polypeptide dry basis and purity basis, 130 to 150 parts of amylum, 5 to 7 parts of lactose, 3 to 5 parts of mannite, 1 to 2 parts of calcium sulphate, 2 to 6 parts of magnesium stearate, 3 to 6 parts of talcum powder, 1 to 3 parts of micro mist silica gel and 2 to 4 parts of tylose. The production methods of the transferring factor are that: the invention firstly concentrates the transferring factor liquor which is evenly mixed with amylum, dried, crushed, and then evenly mixed with the accessories, filled into the capsule to obtain the invention.
CN101781304A Tetrahydroisoquinoline compound and preparation method and application thereof The invention relates to a tetrahydroisoquinoline compound. The tetrahydroisoquinoline compound is of 2-methyl-6,7-methylenedioxy-1-(6-R substituted amino phthalide-3-base)-1,2,3,4-tetrahydroisoquinoline. The general structural formula is: R is Alkyl formyl or substituted or non-substituted Aryl formyl. The invention also provides a preparation method and an application of the tetrahydroisoquinoline compound. The tetrahydroisoquinoline compound has good anti-tumor activity, can be used as new anti-tumor drug so as to bring good news to the tumor patients, has simple preparation and low production cost, and is applicable to the large-scale popularization to use.
US20110294887 Controlled-release solution formulations of pregabalin A controlled-release oral solution formulation, which gels in the stomach, includes pregabalin or a pharmaceutically acceptable salt of pregabalin and a gelling agent.
WO2013169399A1 Oxysterol analogue oxy133 induces osteogenesis and hedgehog signaling and inhibits adipogenesis This invention relates, e.g., to a synthetic compound, Oxy133, having the structure [Formula I] or a bioactive or pharmaceutical composition comprising Oxy133 and a pharmaceutically acceptable carrier. Methods are also disclosed for using the compound or bioactive or pharmaceutical composition to treat a variety of disorders, including e.g. bone disorders, obesity, cardiovascular disorders, and neurological disorders.
CN101074261A TRAIL receptor I and/or TRAIL receptor 2 specific antibody and its use A specific antibody combined TRAIL acceptor 1(TRAIL-R1) and/or TRAIL acceptor 2(TRAIL-R2), its amino-acid sequence and nucleotide sequence for encoding it and its usage in treatment of tumor are disclosed.
US7465744 Triazole compounds and the therapeutic use thereof The invention relates to triazole compounds of general formula (I), wherein A, B, R1, R2, R3 and R4 have the meaning cited in claim 1. The invention also relates to a pharmaceutical agent containing at least one compound of general formula (I) in addition to the use of the compound (I) for producing a pharmaceutical agent for treating illnesses, responding to the effects of dopamine-D3-receptor antagonists or dopamine-D3-receptor agonists, especially for treating disorders in the central nervous system.
WO2007021309A1 Substituted isoindolones and their use as metabotropic glutamate receptor potentiators The present invention is directed to compounds of formula (I), wherein R1 is a ring, R5 is a specified substituent, and n is from 1 to 8. The invention also relates to the use of the compounds in therapy as metabotropic glutamate receptors modulators, particularly in neurological and psychiatric disorders.
US7271163 Cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these compounds and methods for their use, including treatment of obsessive-compulsive disorder, panic disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.
CN101972262A Oral liquid for treating poultry coccidium and bacterium mixed infection and preparation method thereof The invention discloses oral liquid for treating poultry coccidium and bacterium mixed infection and a preparation method thereof, and aims to provide the oral liquid for treating the poultry coccidium and bacterium mixed infection, which is convenient to use and the preparation method thereof. Each 100L of oral liquid comprises the following components: 1 to 5kg of sarafloxacin hydrochloride, 0.2 to 1kg of diclazuril, 2.5kg of ethanolamine, 30L of purified water, 0.5kg of sodium hydroxide, 30kg of dimethyl formamide and the balance of 95 percent ethanol. In the oral liquid of the invention, the diclazuril serves as an anti-coccidium medicament, the sarafloxacin hydrochloride serves as an anti-bacterium medicament, and the coccidium and the bacterium can be resisted at the same time by using the diclazuril and the sarafloxacin hydrochloride together. The oral liquid can be mixed with water in any ratio, is convenient to use, can achieve the effect of commonly treating the coccidium and bacterium mixed infection by the independent application of the oral liquid, reduces situations such as treating opportunity delay caused by diagnostic errors or misdiagnosis, and is convenient for broad culturists.
CN103006577A Application of salvianolic acid A lyophilized powder injection in preparation of drugs for preventing and/or treating cerebral thrombosis The invention relates to application of salvianolic acid A lyophilized powder injection in preparation of drugs for preventing and/or treating cerebral thrombosis. The salvianolic acid A lyophilized powder injection comprises, by weight, 20-60g of salvianolic acid A, 20-60g of filling agent, and an antioxidant accounting for 0.02%-0.1% of the total amount of the finished product.
EP2698157A1 Method of treatment using fatty acid synthesis inhibitors The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as diabetes, and/or diabetes related disorders.
CN101019868A Cream for treating alopecia and its prepn The present invention discloses one kind of cream for treating alopecia. The cream is prepared with minoxidil, stearic acid, glycerol monostearate, white vaseline, propylene glycol, sodium thiosulfate, disodium edta, etc. The present invention adopts propylene glycol as both solvent and transdermal promoter, and sodium thiosulfate and disodium edta as antioxidants to prevent the oxidation of minoxidil, so as to result in even high treating effect. The cream of the present invention has obvious treating effect, no irritation, no hypersensitivity, low cost and other advantages, and is used in treating different kinds of alopecia.
CA2213996C Oral pharmaceutical dosage forms comprising a proton pump inhibitor and an antacid agent or alginate An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more antacid agents or an alginate in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer and an optional separating layer in between the proton pump inhibitor and the enteric coating. The fixed formulation is in the form of multilayered tablets, sachets or multiple unit tableted dosage forms. The multiple unit dosage form is most preferred. The new fixed formulation is especially useful in the treatment of disorders associated with dyspepsia such as heartburn.
CN103127065A Application of Eryngiolide A in medicines reducing blood sugar The invention discloses application of Eryngiolide A in preparation of anti-diabetic medicines. The application of the Eryngiolide A in preparation of anti-diabetic medicines provides a brand new selection and thought for existing anti-diabetic medicines, widens the selecting field of anti-diabetic medicines, and makes great contribution to development of the anti-diabetic medicines technical field. The application of the Eryngiolide A in preparation of medicines reducing blood sugar is proved to have evident anti-diabetic effect, and chooses composition with definite chemical structures. Use of the Eryngiolide A in preparation of medicines reducing blood sugar is made public for the first time, the skeleton type is completely novel, and the Eryngiolide A has an unexpectedly high activity of preventing and curing diabetes, probability of other compounds giving any revelation for the Eryngiolide A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in curing diabets.
WO2007071876A1 Composition of inverse emulsion type comprising ivermectin, and uses thereof in cosmetics and dermatology The present invention relates to a composition comprising at least one compound of the avermectin family, preferably ivermectin, characterized in that the composition is an inverse emulsion containing a glycol or water-glycol dispersed hydrophilic phase, a lipophilic continuous phase and an emulsifier with an HLB of between 2 and 7, wherein said composition does not comprise any DHEA and/or its chemical and/or biological precursors and/or derivatives and/or any vitamin D derivative. This inverse emulsion makes it possible to prevent crystallization of the active agent and/or chemical degradation thereof while at the same time having good stability and being well tolerated.
EP1366036B1 Compounds having activity as inhibitors of cytochrome p450rai Compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
CN1931148A Prepn process of levofloxacin lactate oral film The present invention is preparation process of levofloxacin lactate oral film and belongs to the field of medicine preparing technology. The levofloxacin lactate oral film consists of medicine layer and protecting layer. The medicine layer has matrix comprising PVA and sodium carboxymethyl cellulose in the weight ratio of 2 to 1, and the effective medicine components comprising levofloxacin lactate, dexamethasone acetate and vitamin B2. The protecting layer is PVA. The effective components in the medicine layer may be also bioactive matter lysozyme or antibiotic peptide and vitamin B2. The levofloxacin lactate oral film may be applied directly onto the wound surface of oral cavity ulcer, and has prolonged treating period. The protecting layer can protect the medicine layer against the elution of saliva so as to raise the treating effect.
WO2010109450A1 Rhodamine 6g for use in treating cancerous cells The present invention provides a therapeutic composition for treating a broad range of solid and non-solid tumors at a very low toxicity level. The composition contains microgram levels of the active agent, rhodamine 6G, and is administered systemically or topically.
US7488725 To treat diabetes, especially type II diabetes including complications of diabetes; synergistic Compounds are provided having the formula: wherein R1, R2, R2′, R3, R3′, R4, R4′, R5, X, Y and Z are as defined herein.
CN101721365B Levulose liposome injection and novel application thereof The invention discloses levulose liposome injection and a novel application thereof. The levulose liposome injection comprises 1 part of levulose, 3-20 parts of soybean lecithin, 0.5-8 parts of cholesterol, 0.3-10 parts of poloxamer 188, 0-5 parts of osmotic pressure regulator and 1-5 parts of pharmaceutically acceptable buffer solution.
CN103690487A Carrier-free micro-nano resveratrol medicament and preparation and application thereof The invention discloses a carrier-free micro-nano resveratrol medicament and preparation and application thereof. The carrier-free micro-nano resveratrol medicament is a product prepared by a preparation method comprising the following steps: (1) putting resveratrol powder into a crucible, and calcining in a tubular furnace in the presence of gas protection; (2) after calcining, cooling the tubular furnace to the normal temperature to obtain the micro-nano resveratrol medicament. The micro-nano resveratrol medicament has the advantages that (1) no carriers or organic solvents are contained, so that the medicament content is up to 100 percent; (2) the defects of low water solubility and low bioavailability are overcome, the product is needle-shaped or strip-shaped, the width is 0.2-0.5 mu m, and the solubility of the product in water is 30-50mumol/L; (3) the IC50 (50% inhibitory concentration) value of the product to a human hepatoma cell HeLa is 0.1-0.2 mu mol/mL, and the IC50 value to a human hepatoma cell HepG2 is 0.2-0.3 mu mol/mL.
US7547730 Preventive and/or therapeutic treatment of hyperlipidemia or non-insulin dependent diabetes mellitus which comprises dministering orally a polyprenyl compound 3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid (NIK-333); antidiabetic and -lipemic agents Activators of peroxisome proliferator-activated receptors comprising a polyprenyl compound, preferably (2E,4E,6E,10E)-3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid, as an active ingredient, and medicaments for preventive and/or therapeutic treatment of hyperlipidemia, non-insulin dependent diabetes mellitus or the like comprising a polyprenyl compound as an active ingredient.
CN102846656A Skin mucosa disinfecting liquid and preparation method thereof The invention discloses skin mucosa disinfecting liquid and preparation method thereof. The skin mucosa disinfecting liquid contains (by weight ratio) chlorhexidine acetate 0.25% plus or minus 0.02%, benzalkonium bromide 0.0125%, sodium nitrite 0.015%, glutaraldehyde 0.02%, octyl phenoxy poly ethoxy 0.05%, and residual amount of distilled water. Using octyl phenoxy poly ethoxy for assisting dissolution and containing no alcohol substances such as glycerol, the invention has little irritation on skin mucosa. The invention has wide application scope, and can be used for sterilization of oral mucosa, pudendum, skin mucosa and damaged skin and for mucosa sterilization in medical institution.
US20110160260 Method of Treating a Neurodegenerative Disorder The present invention provides a method of treating a neurodegenerative disorder in a patient, comprising administration to the patient a therapeutically effective amount of D-cycloserine and its derivatives.
CA2836131A1 Synergistic combinations of polyene fungicides and non-ribosomal peptides and related methods of use The present invention includes compositions comprising a synergistic fungicidal combination of a polyene fungicide and at least, one lipopeptide and methods for using such compositions in controlling fungal pathogens.
EP2460517A1 Reducing risk of type 2 diabetes (T2D) This invention relates to methods for reducing chronic subacute inflammatory states associated with obesity and improve glycaemia, thereby preventing or delaying the development of type 2 diabetes (T2D) in obese subjects, or subjects with metabolic syndrome, using non-acetylated forms of salicylate, for example salsalate or trilisate.
US20130018064 Amino Heteroaryl Compounds as Beta-Secretase Modulators and Methods of Use The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I, wherein ring A, B1, B2, B3, L, R1, R4, ring Z, m and p of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
US20090163555 Isolated optically active stereoisomers are useful for enhancing an immuneresponse, for treating autoimmune diseases and asantitumor agents, bacteriacides, fungicides or viricides; one pot synthesis of1-(3-a3S,5R-1-(3-amino-5-carboxy-2-oxopyrrolidin-3-ylmethyl)pyridinium bromide hydrobromide Novel pyroglutamic acid derivatives (I), wherein R1 is —OH, —ORa, wherein Ra is alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl or heterocyclyl; R2, R3 and R4 are independently H, a nitrogen protecting group which hydrolyzes under acidic conditions or phtalamide; X is a pharmaceutically acceptable anion; and Y is a N-containing group; either in the form of their isolated optically active stereoisomers or in the form of mixtures thereof, are useful compounds for enhancing an immuneresponse in a subject and/or for treating tumours, bacterial, fungal or viral infections, or autoimmune diseases.
CN101716135B Soy isoflavone solid dispersion suppository and preparation method thereof The invention discloses a soy isoflavone vaginal suppository and a preparation method thereof. Raw materials for preparing the suppository comprise soy isoflavone solid dispersion and a water-soluble substrate, wherein the soy isoflavone solid dispersion is prepared from soy isoflavone and a hydrophilic solid dispersion carrier, and the mass ratio of the soy isoflavone and the carrier is 1:1-20. The invention designs and prepares a soy isoflavone solid dispersion suppository for vaginal drug administration on the premise of overcoming the defect of poor absorption effect of the oral administration of the soy isoflavone. The solid dispersion technology improves the dispersity and the hydrophilism of the soy isoflavone and improves the moisture degree on the vagina mucosa, thereby improvingthe infiltration rate of the prepared suppository by 2-3 times. The suppository greatly improves the curative effect of the soy isoflavone on treating and mitigating a series of diseases of women caused by maladjustment of estrogen level.
CN102125544A Inducer for activating expression of fish lipid metabolism control gene and application thereof The invention discloses an inducer for activating the expression of a fish lipid metabolism control gene and application thereof. The inducer is prepared from one or a mixture of more of clofibrate, 2-palmitic acid, 15-deoxidized-delta 12 and 14-prostaglandin J2. The inducer can activate the expression of the fish somatic cell lipid metabolism control gene, namely a peroxisome proliferator activated receptor gene, so that the inducer can be used for breeding fishes, maintaining the nutrition metabolization balance in the fish breeding, reducing lipidosis of the fishes and improving the quality of fish flesh.
WO2007013062A1 Composition and method for weight maintenance The present invention relates to a composition and method for weight maintenance. Specifically, the composition of the invention which comprises sebacoyl bis-sarcosine (SBS) is useful in maintaining weight in individuals with a history of obesity or those having a risk of becoming obese.
US20110033418 Treatment of diseases caused by viral infection A method of prophylactic and/or therapeutic treatment of a mammal is provided for treating a disease that is caused by a Ljungan virus infection. The method comprises administration to the mammal of an antivirally effective amount of ribavirin or a derivative thereof effective against the Ljungan virus and pleconaril or a derivative thereof effective against the Ljungan virus to eliminate or inhibit proliferation of said virus in said mammal and at the same time prevent and/or treat said disease in said mammal. Also provided is a composition comprising ribavirin or a derivative thereof effective against a Ljungan virus and pleconaril or a derivative thereof effective against a Ljungan virus and a kit relating to this composition. Further, a method is provided for treating Ljungan virus infection comprising administering ribavirin or a derivative thereof effective against the Ljungan virus as well as a composition and a kit comprising ribavirin.
EP2617429A1 Fat oxidation or energy metabolism enhancer A composition, a pharmaceutical product, a quasi-drug, a food, a drink, a pet food, a feed, and the like which are highly safe and have excellent facilitatory actions on fat oxidation or energy metabolism are provided. Also disclosed is a roasted coffee bean extract for use in enhancement of fat oxidation or energy metabolism, comprising chlorogenic acids or salts thereof and having the content of hydroxyhydroquinone of less than 0.1% by mass relative to the content of the chlorogenic acids. Further disclosed is use of a roasted coffee bean extract for the production of a fat oxidation or energy metabolism enhancer, comprising chlorogenic acids or salts thereof and having the content of hydroxyhydroquinone of less than 0.1% by mass relative to the content of the chlorogenic acids.
US8759097 Inhibition of dynamin related protein 1 to promote cell death The present invention relates to compositions and methods for reducing cell proliferation and/or promoting cell death by inhibiting Drp1. It is based, at least in part, on the discoveries that (i) Drp1 disruption-induced mitochondrial hyperfusion is functionally linked to the cell cycle regulation apparatus, so that Drp1 inhibition results in a disruption of the cell cycle and DNA aberrancies; (ii) inhibition of both Drp1 and ATR are synthetic lethal causing increased DNA damage and apoptotic cell death; and (iii) even in resistant cell lines, Drp1 inhibitor (e.g., mdivi-1) together with a second antiproliferative agent (e.g., cisplatin or carboplatin) act synergistically to promote apoptosis. Accordingly, the present invention provides for novel anticancer strategies.
CN103664623A Application of depside derivatives The invention provides application of compounds or pharmaceutically acceptable salts shown as the general formula I, and application of pharmaceutical compositions and plant extract products both containing the compounds or the pharmaceutically acceptable salts. The compounds or pharmaceutically acceptable salts of the general formula I, the pharmaceutical compositions and the plant extract products are capable of increasing the transcription of lipoprotein lipase in adipocyte in cell level, thereby improving lipid metabolism. Therefore, the compounds or pharmaceutically acceptable salts of the general formula I, the pharmaceutical compositions and the plant extract products are applicable to prepare medicines for treating II type diabetes and hypertriglyceridemia.
CN102603910A Preparation method of pachyman sulfate The invention discloses a preparation method of pachyman sulfate. The preparation method comprises the following steps of: adding sulfamic acid and an organic solvent in a reaction bottle of a rotary evaporator; preheating to reaction temperature; after fully dissolving the sulfamic acid, adding dried pachyman powder; vacuuming a reaction system; cooling to room temperature after the reaction is finished; adjusting the pH of reaction solution to 9-10 with saturated alkali solution; continuously vacuuming to remove ammonia and repeatedly vacuuming until the reaction solution has no ammonia smell; maintaining the pH value to be over 7 until the pH value does not go down; then adding ethanol; precipitating polysaccharide sulfate; filtering and then dissolving in water again; filtering; placing in an ultrafilter to desalinate and concentrate; and detecting residual quantity of free sulfate radicals in eluent by using saturated barium chloride solution until no white precipitate is produced. According to the preparation method, the sulfation efficiency is greatly increased, polysaccharide molecule degradation and production of sugar ring double ring are suppressed, the color of a product becomes light, and the final quality of the product is obviously improved.
EP1187837B1 Thiazepine inhibitors of hiv-1 integrase The present invention discloses non-catechol compounds, such as thiazolothiazepines, and analogs and derivatives thereof, which are anti-integrase inhibitors. The compounds, which are useful as treatments for HIV disease, include compounds (I), (II), (III), or pharmaceutically acceptable salts thereof wherein A is thiazole, benzene, naphthalene, pyridine, pyrimidine, pyrazine, or quinoline; R is one or more of H, halogen, lower alkyl, lower alkoxy, NO2, lower ester or carboxylic acid; X-Y is CH2-S, S-CH2, CH2-O, CH2-S(O), S(O)-CH2, CH2-CH2, CH2-CH2-CH2, or CH2-CH2-CH2-CH2; R4 is H or hydroxy; R5 is H, phenyl, or alkylamine; W is S or O; and R6 is H, substituted or unsubstituted alkyl or amine; and Z is S, O, CH2, CH2CH2, or C=O.
US20060293221 Mucosal repair by TFF2 peptides The present invention relates to the use of trefoil factor 2 (TFF2) peptides and a pharmaceutical composition comprising TFF2 peptides for increasing the viscosity of mucin in mucus layers and the repair of damaged mucus layers in the gastrointestinal tract (mouth, oesophagus, stomach, small and large intestine, colon) the respiratory passages, the eye, the urinary system (including the bladder) and the cervis uteri.
US8192753 pH-sensitive cationic lipids, and liposomes and nanocapsules containing the same The invention suggests a pH-sensitive cationic lipid with a pKa value between 3.5 and 8, according to the general formula cation-spacer-Y-spacer-X-lipid, wherein Y and X represent linking groups. Furthermore, liposomes are described, which liposomes include said optionally cationic lipids.
CN101797251A Inhibitor for acetylcoenzyme A synthetase in human pathogen clostridium difficile The invention belongs to the technical field of biological medicine, and specifically provides a human pathogen clostridium difficile inhibitor taking acetylcoenzyme A synthetase (ACS) as a target. This invention utilizes a fast reaction kinetics technique to successfully find an acetylcoenzyme A synthetase inhibitor with high inhibitory activity, which comprises 1,10-o-phenanthroline, 2,2-bipyridyl and 8-hydroxyquinoline, wherein the conventional clinically applied medicament, namely 8-hydroxyquinoline, can inhibit methyl transfer activity of acetylcoenzyme A nearly by 100 percent in a low concentration. A method of the invention is the only reported method at present for an efficient inhibitor of human pathogen clostridium difficile acetylcoenzyme A synthetase. The inhibitor is of important application value in the field of biological medicine.
CN103054877A Composition containing alisol A and application of composition containing alisol A on medicine The invention discloses a composition containing alisol A and an application of the composition containing alisol A on medicine, and the composition containing alisol A comprises the following ingredients by weight, alisol A: alisol A-23-acetate: alisol A-24-acetate is 1: 0.05-0.3: 0.05-0.5. The composition has the advantages of stable quality and high security, compared with single administration of alisol A or alisol A-23-acetate or alisol A-24-acetate, the composition containing alisol A with long-time administration has better hypolipemic effect by using same dosage with the alisol A or alisol A-23-acetate or alisol A-24-acetate, and in-vitro hepatotoxicity test results display that compared with single administration of alisol A or alisol A-23-acetate or alisol A-24-acetate with same dosage, the composition presents weak performance on cytotoxicity of hepatocyte. The alisol A-23-acetate combines with alisol A or alisol A-24-acetate to obtain the composition, the stability of alisol A-23-acetate is obviously increased, and the druggability is enhanced.
WO2009000853A2 Combination formulations comprising darunavir and etravirine This invention relates to solid oral dosage forms of the HIV inhibitors containing a combination of TMC114 and TMC125.
US7259159 Vitronectin receptor antagonists for treating and preventing osteoporosis, bone disorders The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical compositions comprising them
WO2005115998A1 TYROSINE DERIVATIVES SUBSTITUTED BY ALKANOYLAS hPPARα & hPPARϜ ANGONISTS The invention provides compounds of the general formula (I), racemic mixtures, optical isomers, pharmaceutically acceptable salts, solvates and pharmaceutical compositions thereof. The definitions of substituents in the general formula (I) are the same as the definitions of claims. The present invention also relates to the preparation for the compounds of the general formula (I) and the usage thereof for the preparation of a medicament, which is used for treating hyperglycemia, lipidosis lipaemia and NIDDM (type II) diabetes.
CN101015342A Preparation method of lycopersicin microcapsule The invention relates to a method for preparing lycopene microcapsule, belonging to food engineering technique. It comprises following steps: (1) putting compound emulsifier and water into solid lycopene powder, grinding in ball grinder to form emulsion; (2) dissolving wall material into water, stirring and getting wall material solution; (3) mixing said lycopene emulsion with wall material, homogenizing with colloid mill; (4) spray drying homogenized mixing liquid and getting lycopene microcapsule. The invention is characterized by simple process, no organic solvent residual, high productivity, and suitability for large production. The produced lycopene microcapsule is characterized by sphere shape, pink color, homogenous granular size, smooth surface, no smelly odor, good fluidity, good water solubility, high content of lycopene, restoration at normal temperature and packed with polyethylene film bag of 0.2mm, and long storage period of more than 4 months.
CN101955442A Benzoyl fluorobenzene salicylamide compound and application thereof The invention discloses an N-(4-nitro-3-trifluoromethanephenyl)-benzoyl fluorobenzene salicylamide compound shown as the formula (I) and application thereof in preparing anti-tumor medicaments, especially medicines for resisting endometrial cancer and lung cancer. The N-(4-nitro-3-trifluoromethanephenyl)-benzoyl fluorobenzene salicylamide compound and the application thereof have the advantages of providing a new anti-tumor medicament with obvious anti-tumor activity, providing a research foundation for new drug screening and having significant application prospect.
CN101856393A Application of compound Yiganling composition in aspect of auxiliary treatment of chemotherapy of tumors The invention discloses application of a compound Yiganling composition in the aspect of the auxiliary treatment of the chemotherapy of tumors. The functions are the function of synergy and toxicity reduction to the chemotherapy of the tumors, the function of relieving bone marrow suppression caused by chemotherapeutic medicines, the function of relieving leukopenia caused by the chemotherapeutic medicines, the function of alleviating the pathological injury of the tissues of the liver and the kidney, the function of promoting the regeneration of stem cells and the function of sensitivity enhancement to multi-medicine resistance caused by the chemotherapeutic medicines.
US6875576 Detection of modulators of receptor binding activity; obtain sample containing receptor, incubate with modulator, monitor adjustment of binding activity of receptor The present invention relates to in vitro methods for evaluating compounds that better correlate with therapeutic efficiency than evaluating compounds based on potency alone. In general, the inventive method comprises: (i) determining a potency value for a compound against its target receptor; (ii) determining a desensitization value for the compound against its target receptor; and (iii) comparing the potency value with the desensitization value. If the desired action of a compound is as a receptor agonist, then the compound's desensitization value should be larger than the compound's potency value. This ensures that the concentration of a compound required for potency will not also cause the receptor to desensitize at the same time, thus in an essence nullifying the desired effect. The inventive methods are used to evaluate novel motilide compounds as well as ABT-229 and EM-574, two motilide compounds for which clinical trials have been initiated.
US20070287728 Novel Naphthyl Substituted Azabicyclo Derivatives and Their Use as Monomine Neurotransmitter Re-Uptake Inhibitors This invention relates to novel naphthyl substituted azabicyclo derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
US20110152351 Modulation of smrt expression Disclosed herein are compounds and methods for decreasing SMRT and treating metabolic and/or cardiovascular diseases in an individual in need thereof. Examples of disease conditions that can be ameliorated with the administration of antisense compounds targeted to SMRT include obesity, diabetes, dyslipidemia, and hypothyroidism.
WO2009105162A3 Hsp90 inhibitors or modulators for treatment or prevention of substance-related disorders The present disclosure provides methods of treating or preventing a substance-related disorder using Hsp90 inhibitors, Hsp90 modulators, tyrosine hydroxylase modulators, and modulators that reduce the interaction between Hsp90 and tyrosine hydroxylase.
EP1263757B1 Benzthiazoles as tnf and pde-iv inhibitors Compounds that are inhibitors of phosphodiesterase and have therapeutic utility, are of formula (i) wherein R1 is C3-6 cycloalkyl, or C1-3 alkyl optionally substituted with one or more fluorine atoms; R2 is C1-6 alkyl, C3-6 cycloalkyl, CF3, CH2CF3, C2F5 or NR4R5; R3 is pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, are each H, C1-3 alkyl, halogen, CF3 or CN, provided that both are not H; or a pharmaceutically-acceptable salt thereof.
CN101768079A Compound and medicinal application thereof The invention discloses a newly-discovered compound and medicinal application thereof. The newly-discovered compound is characterized in that the new compound with good stability and membrane permeability and high bioavailability can be screened by reforming the structure of salvianolic acid A in salvia sclarea and carrying out stability experiment, Lop determination, pharmacodynamic experiment and the like and has better pharmacological effects in the aspect of treating cardiovascular and cerebrovascular diseases and other diseases.
US20080261908 Adverse prognostic markers estrogen receptor, progesterone receptor expression, positive lymph node metastasis, high proliferative index, detectable p53 expression; identify breast cancer-specific signature of miRNAs differentially-expressed in breast cancer cells relative to normal control cells The present invention provides novel methods and compositions for the diagnosis, prognosis and treatment of breast cancer. The invention also provides methods of identifying anti-breast cancer agents.
US20080241231 Transdermal delivery of dexamethasone and promethazine Relief or prophylaxis from nausea and/or emesis are provided by transdermal compositions comprising dexamethasone and promethazine. The transdermal compositions are in the form of transdermal solutions and/or suspensions, such as lotions, pastes, gels, ointments or transdermal patches.
WO2013082565A1 Therapies for disorders of the cornea and conjunctiva Unexpectedly, disorders of the cornea and conjunctiva are found to be caused or to be exacerbated, at least in part, by extracellular ATP and P2X7 receptor activation. Therapeutic compositions for topical administration to the eye for the treatment of disorders of the cornea and conjunctiva include an entity that inhibits P2X7 receptor function, reduces the effective concentration of extracellular ATP, or both.
CN103463078A Application of Lycojaponicumin C in medicine for treating kidney cancer The invention discloses an application of Lycojaponicumin C in preparation of a medicine for treating kidney cancer, belonging to the technical field of a new application of a medicine. The invention discovers that Lycojaponicumin C has the remarkable inhibitory effects on the growth of human kidney cancer cell strain KC through the evaluation of in vitro MTT (methyl thiazolyl tetrazolium) antineoplastic activity. Therefore, Lycojaponicumin C can be used for preparing the kidney cancer resisting medicine and has good development and application prospects. The application of Lycojaponicumin C in preparation of the medicine for treating kidney cancer, related to the invention, is disclosed for the first time. The skeleton type is a brand-new one, and the inhibitory activity of Lycojaponicumin C on kidney cancer cells is unexpectedly strong.
US7253151 Genes of IL-12P40 subunit mutated for improving the activity of IL-12 and use thereof for DNA vaccine adjuvant The present invention relates to the IL-12p40 subunit mutant gene which can produce IL-12(interleukin 12) of human and mouse origin with high activity, the expression vector including above mutant gene and the use of them to DNA vaccine adjuvant. Particularly, it relates to IL-12p40 mutant gene which inhibits the secretion of IL-12p40 but normally secretes active IL-12p70 by making mutation at Asn-222(human) or Asn-220(mouse) amino acid of IL-12p40, which acts as a competitive inhibitor of active form of IL-12, IL-12p70. Therefore, the IL-12p40 mutant gene of the present invention can be useful for DNA vaccination and gene therapy against various diseases, for example, AIDS, hepatitis C or hepatitis B, cancer, influenza, tuberculosis and malaria, which essentially require cellular immune responses for their therapy.
EP1792902A1 Processes for preparation of 5-(6-quinazolinyl)-furan-2-carbaldehydes Ditosylate salts of 4-quinazolineamines are described as well as processes for their preparation, and methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity.
CN101623271B Compound alpha-keto acid dispersible tablet The invention discloses a compound alpha-keto acid dispersible tablet for treating chronic kidney diseases, containing four kinds of keto amino acid calcium, one kind of hydroxyamino acid calcium, five kinds of amino acid and pharmaceutically acceptable adjuvants. The tablet is mainly and clinically used for postponing renal failure process, correcting metabolic disturbance, coordinating with low-protein diet and preventing and treating damages caused by protein metabolism disorder because of chronic renal insufficiency.
WO2012168721A1 Materials and methods for treating pten mutated or deficient cancer The use of inhibitors of mitotic kinases, such as TTK protein kinase, is described for use in the treatment of cancers which are characterized as Phosphatase and Tensin Homolog (PTEN) mutated or deficient cancers.
WO2009041640A1 Plant extract and use thereof Disclosed is a plant extract which contains an o-diphenol-type chlorogenic acid component at a high concentration. Also disclosed is a plant extract which contains substantially no feruloyl quinic acid component or caffeine component, and which has an excellent deodorant or anti-oxidative property. A plant extract which contains a chlorogenic acid component comprising o-diphenol-type chlorogenic acid, and which contains substantially no feruloyl quinic acid component or caffeine component has an excellent deodorant or anti-oxidative property.
CN102847075A Medicine composition for treating insomnia The invention relates to medicine composition for treating insomnia, which consists of following ingredients in parts by weight: 15 to 35 parts of Chinese angelica, 10 to 30 parts of roots of red-rooted salvia, 15 to 30 parts of radix curcumae, 10 to 25 parts of polygala tenuifolia, 5 to 23 parts of liquorice, 10 to 28 parts of poria with hostwood, 15 to 33 parts of fried spina date seeds, 1 to 15 parts of fructus alpiniae oxyphyllae, 5 to 23 parts of pericarpium citri reticulatae, 4 to 22 parts of platycladi seeds, 6 to 24 parts of calamus, 5 to 23 parts of dragon bone, 15 to 33 parts of rheum officinale, 1 to 15 parts of ligusticum wallichii, 2 to 18 parts of schisandra chinensis, 5 to 23 parts of radix paeoniae alba, 2 to 18 parts of Cape jasmine, 10 to 28 parts of cortex albiziae, 0.4 to 0.7 part of propranolol hydrochloride, 0.4 to 0.7 part of oryzanol and 0.2 to 0.3 part of diazepam tablets. The medicine composition has a function for treating nervous insomnia caused by various reasons, refractory insomnia and insomnia with unknown reasons; and moreover, the medicine composition is remarkable in curative effect, short in treatment process, fast in effectiveness and free from side effect.
EP1011743B1 Loading and release of water-insoluble drugs A medical device, polymer composition, and method for delivering substantially water-insoluble drugs to tissue at desired locations within the body. At least a portion of the exterior surface of the medical device is provided with a polymer coating. Incorporated in the polymer coatings is a solution of at least one substantially water-insoluble drug in a volatile organic solvent. The medical device is positioned to a desired target location within the body, whereupon the drug diffuses out of the polymer coating.
CN102247328A Salidroside freeze-dried powder injection and preparation method thereof A salidroside freeze-dried powder injection and a preparation method thereof relate to a freeze-dried powder injection prepared by salidroside and a preparation method thereof. Research finds that common stonecrop herb has a plurality of efficacy and functions which mainly comprise the following various pharmacological effects: anti-hypoxia, anti-fatigue, anti-shock, anti-aging, anti-tumor, cardiac cerebral function improvement, and the like. The invention relates to a salidroside freeze-dried powder injection which is prepared by 1-10 parts by weight of chemically-synthesized salidroside and 1-10 parts by weight of pharmaceutic adjuvants. The injection of the invention is applicable to the treatment of various shock and cardio-cerebrovascular diseases.
CN101869552B Preparation method of chitin tablet The invention relates to a preparation method of a chitin tablet. Chitin raw material is smashed and screened with a 60 mesh sieve and then 3 percent of HPMC and 6 percent of starch, which are used as adhesives, are added to prepare soft material. A 16 mesh net is used for granulating, and the obtained granules are dried, smashed and then screened through a 100 mesh sieve. A certain amount of calcium hydrophosphate, dextrin, talcum powder and magnesium stearate are added to the smashed fine powder and then are mixed evenly through a blender mixer. The tablet with certain specification is manufactured according to the requirement. The chitin prepared through the method accords with the quality requirement of the common tablet.
WO2009058361A1 Inhibition of type i ifn production The invention provides methods for decreasing type I IFN production by human plasmacytoid dendritic cells in response to TLR activation.
CN101380327A Anti-cancer composite sustained-release composition and preparation method thereof The invention provides an anticancer compound slow release composite and a preparation method thereof. All or part of an anticancer synergist and a side effect lightening admixture are made into a slow release part to enhance the effect of the anticancer agent and lower the toxic and side effect on the stomach and intestine.
EP1997496A1 Composition containing riboflavin and sesamins The present invention relates to a composition containing riboflavin and a sesamin-class compound(s). This composition may incorporate a sesamin-class compound(s) in such an amount that the proportion (weight ratio) of its total quantity to the total quantity of riboflavin taken as unity is no more than 4.5, and it has the advantage that the analgesic and anti-fatigue actions of riboflavin are synergistically improved by ingestion of riboflavin in combination with a sesamin-class compound(s). The composition of the present invention provides compositions, in particular, pharmaceuticals as well as foods and beverages that are safe to humans, animals, etc. and can therefore be ingested for a continued period, and which have far superior effects to those of conventional foods having an analgesic or anti-fatigue action.
WO2014073659A1 Oral administration composition for ameliorating or preventing hypertension The purpose of the present invention is to provide an oral administration composition for ameliorating or preventing hypertension. The oral administration composition for ameliorating or preventing hypertension in a daily dosage for Japanese patients, said composition being processed into an orally administrable form, is produced by preparing a mixture of materials capable of providing 1,500-2,000 kcal of total energy (per day, the same will apply hereinafter), 180-200 mg of cholesterol, 2,800-3,500 mg of sodium, 3,600-4,400 mg of potassium, 810-990 mg of calcium, 360-440 mg of magnesium and 22.5-27.5 g of dietary fiber, and dividing the mixture into multiple portions for daily administration.
CN102174048A Novel polymorphic form beta of soporifics The invention relates to a method for preparing polymorphic form beta of N-methyl-N-(3-(3-[2-thienylcarbonyl]-pyrazol-[1,5-alpha]-pyrimidine-7-radical)phenyl)acetamide. The invention also relates to application of the polymorphic form beta of N-methyl-N-(3-(3-[2-thienylcarbonyl]-pyrazol-[1,5-alpha]-pyrimidine-7-radical)phenyl)acetamide used as a sedative-hypnotic drug, an anxiolytic drug, an anticonvulsive drug and/or a skeletal muscular relaxant. The polymorphic form beta of N-methyl-N-(3-(3-[2-thienylcarbonyl]-pyrazol-[1,5-alpha]-pyrimidine-7-radical)phenyl)acetamide has the advantages of simple preparation method, easiness in operation, capability of obtaining a pure sample at high yield, favorable stability, obvious sedative-hypnotic, anxiolytic and skeletal muscular relaxant effects, and the like.
WO2009024613A1 Tetracyclic indolopyridines as eg5 inhibitors Compounds of a certain formula (I), in which R1, R2, R3 and R4 have the meanings indicated in the description, are effective Eg5-inhibiting compounds with anti-proliferative and/or apoptosis inducing activity.
US20120142784 Lysine-specific demethylase 1(lsd1) is a biomarker for breast cancer The present invention relates to novel biomarker for breast cancer, namely LSD1 and its application in inter alia the diagnosis of breast cancer. Furthermore, the present invention discloses a method of determining the LSD1 protein amount and the effect of LSD1 inhibitors on cancer cells selected from breast cancer, lung carcinoma and sarcoma.
US20100080768 Compositions and Methods for the Treatment of Inflammatory Dermatosis and Other Pathological Conditions of the Skin The present invention relates to a composition used as a vehicle for percutaneous absorption of Pharmaceutical and Cosmaceutical active agents that comprises Dimethiconol (hydroxyl-terminated polydimethydimethylsiloxane), dimethicone-350 (polydimethylsiloxane-350), cyclomethicone-5 nf (decamethylcyclopentasiloxane), alkymeth siloxane copolyol-lauryl peg/ppg 18/18 methicone (alkymethyl siloxane copolyol), cyclopentasiloxane and dimethicone Crosspolymer (silicone elastomer and decamethylcyclopentasiloxane), stearoxytrimethylsilane and stearyl alcohol (silicone wax), and deionized water. This composition serves several key applications: (1) it is a vehicle for percutaneous absorption of Pharmaceutical and Cosmaceutical active agents; (2) it acts as a method for utilizing other compositions in the treatment of inflammatory conditions of the skin including, but by no means limited to, atopic dermatitis (eczema), allergic contact dermatitis, seborrheic dermatitits, psoriasis, xerosis and atopia; (3) it is a treatment of inflammatory conditions of mucosae; (4) it relates to other compositions and methods for protecting and enhancing the barrier function of the skin.
EP0800829B2 Use of a pm-1 antibody or of a mh 166 antibody for enhancing the anti-tumor effect of cisplatin or carboplatin A potentiator for antitumor agents, for example, platinum compounds such as cisplatin and carboplatin, mitomycin C, etc., which comprises an interleukin-6 (IL-6) antagonist such as an antibody against IL-6, an antibody against IL-6 receptor, an antibody against protein gp130, etc.
US20090215814 Method of inhibiting neurotrophin-receptor binding The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.
EP1370549A4 Methods for the preparation of mirtazapine intermediates The preparation of 1-(3-carboxypyridyl-2)-4 methyl-2-phenylpiperazine dihydrate and other mirtazapine intermediates are described. These compounds are particularly useful in the preparation of mirtazapine.
US20100113433 N-Substituted Thiomorpholine Derivatives as the Inhibitors of Dipeptidyl Peptidase IV and the Pharmaceutical Uses Thereof The present invention relates to N-Substituted thiomorpholine compounds of formula I, the possible isomers, the pharmaceutically acceptable salts, the solvates, the hydrates or the prodrugs thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV); and to a method for preparing the compounds of formula I, pharmaceutical compositions comprising the compounds of formula I and use of the compounds of formula II in medical field, particularly in the preparation of medicaments for treating and preventing diabetes (in particular type II diabetes), hyperglycemia, X syndrome, hyperinsulinemia, obesity, atherosclerosis and all kinds of diseases modulated by immune system.
CN103735514A Polyethylene glycol vitamin E succinate and calprotectin modified nanoparticle and preparation method thereof The invention discloses polyethylene glycol vitamin E succinate and calprotectin modified nanoparticle and a preparation method thereof. The polyethylene glycol vitamin E succinate and calprotectin modified nanoparticle is prepared from the following raw materials in parts by weight: 1 part of active medicine, 20 to 40 parts of phospholipid, 2 to 4 parts of sophorolipid, 1 to 2 parts of calprotectin, and 5 to 10 parts of polyethylene glycol vitamin E succinate. Compared with the prior art, the nanoparticle modified by olyethylene glycol vitamin E succinate, sophorolipid and calprotectin has the advantages that (1) the preparation process is simple and controllable; (2) the stability of the nanoparticle is greatly improved, and the nanoparticle can be stabilized in a solution for up to 6 months; (3) a freeze-drying protective additive is not needed for freezing and drying; the obtained freeze-dried powder dissolved again shows small change on particle size and polydispersity index compared with freeze-dried powder without being dissolved; (4) the targeting for tumor cells is enhanced.
WO2011051814A1 Novel crystalline forms of (3r,6r) -3- (2, 3 -dihydro- 1h- inden- 2 -yl) - 1 - [ (1r) - 1 - (2, 6 - dimethyl - 3 - pyridinyl) - 2 - (4 -morpholinyl) -2-oxoethyl] -6- [(1s) - 1 -methylpropyl] -2,5- piperazinedione Disclosed are crystalline forms of (3R, 6R)-3-(2,3-dihydro-1 H-inden-2-yl)-1-[(1 R)- 1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1 S)-1-methylpropyl]-2,5- piperazinedione benzenesulfonate salt and pharmaceutical compositions thereof. Also disclosed are processes for the preparation the above compounds and methods for use thereof.
US20120295962 Targeting micrornas for the treatment of liver cancer Provided herein are methods for the treatment of liver cancer. These methods encompass the administration of a compound comprising a modified oligonucleotide, wherein the modified oligonucleotide is targeted to a miRNA. Also provided herein are compositions for the treatment of liver cancer. Such compositions include compounds comprising a modified oligonucleotide, wherein the modified oligonucleotide is targeted to a miRNA. Certain miRNAs have been identified as overexpressed in liver cancer, such as, for example, hepatocellular carcinoma, and are thus selected for targeting by modified oligonucleotides. Further, certain miRNAs have been identified as overexpressed in hepatocellular carcinoma cells exposed to dioxin, and are thus selected for targeting by modified oligonucleotides. Antisense inhibition of certain of these miRNAs has been found to inhibit cell proliferation and induce apoptosis.
US20050143361 Compositions for pulmonary administration An inhalation medicament comprising orazipone and a beta2-adrenoreceptor agonist and/or a corticosteroid as a combined preparation. Optionally the medicament also comprises one or more pharmaceutically acceptable additive, diluents or carriers. The beta-2adrenoreceptor agonist and the corticosteroid may comprise, respectively, formoterol and budesonide.
CN102058616B Application of soracan gum used as medicine for preventing and treating astriction The invention discloses application of soracan gum used as a medicine for preventing and treating astriction. The soracan gum can be orally taken directly or taken with other food, and because the soracan gum is expanded by sucking water in the human intestinal tract and cannot be absorbed by the intestinal tract, the volume of excrement is added, the gastrointestinal peristalsis is stimulated, the quantity, the weight and the moisture content of the excrement are improved, the excrement defecation speed is accelerated and the astriction is improved. The preparation of the soracan gum has theadvantages of simpleness of operation and process and low cost, and is suitable for industrial production. The soracan gum has the advantages of strong water sucking capability, security and no toxicity, and can effectively stimulate the gastrointestinal peristalsis and improve the astriction phenomenon.
US20130274247 Mirtazapine as an Appetite Stimulant for Cats Methods for stimulating appetite in cats in need thereof are disclosed.
EP1651287B1 Injectable composite for the magnetocytolysis of bone metastatic cells The invention relates to a degradable, biocompatible material which is made from a phosphocalcic cement comprising magnetic particles. Said material can be used to treat bone metastases by means of thermolysis and/or to mark cancer cells.
US20090275557 Novel Composition for Treatment of Diseases Related to Activated Lymphocytes The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists.
CN103405410A Application of Chukrasone B in medicine for treating gastric cancer The invention discloses application of Chukrasone B in preparation of a medicine for treating gastric cancer, and belongs to the technical field of new application of medicines. The in-vitro MTT (3-4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) antitumor activity evaluation shows that Chukrasone B has remarkable inhibition effect on the growth of human gastric cancer cell lines HGC-27, MGC-803, BGC-823 and SGC-7901, so that Chukrasone B has a good development and application prospect and can be applied to the preparation of the medicine for treating gastric cancer. The application of Chukrasone B in the preparation of the medicine for treating gastric cancer is disclosed for the first time; the framework type of Chukrasone B is brand new; Chukrasone B brings unexpected inhibition activity for gastric cancer cells.
CN103142573A Application of salvianolic acid A freeze-dried powder to preparation of drug for improving symptom of neurological function after cerebral ischemia The invention relates to application of a salvianolic acid A freeze-dried powder to preparation of a drug for improving symptom of neurological function after cerebral ischemia. The salvianolic acid A freeze-dried powder contains a salvianolic acid A main ingredient, a filler and an antioxidant in the following weight proportion: 20g-60g of the salvianolic acid A main ingredient, 20g-60g of the filler and the antioxidant accounting for 0.02%-0.1% of the total amount. The salvianolic acid A main ingredient comprises 94%-97% of salvianolic acid A, 0.2%-1.5% of lithospermic acid, 0.2%-1.5% of rosmarinic acid, 0.2%-1.5% of salvianolic acid B and 0.4%-2% of salvianolic acid C.
US20060111553 Novel thrombin inhibitors, the preparation and use thereof Compounds of the formula and the salts thereof with physiologically tolerated acids and the stereoisomers thereof, in which the substituents have the meanings stated in the description, are described. Also disclosed are intermediates for their preparation. The compounds are suitable for controlling diseases.
US7087648 Methods for modulating macrophage proliferation using polyamine analogs Methods for modulating macrophage proliferation in an individual afflicted with or at risk for a macrophage-associated disease are provided. The methods employ a polyamine analog, or salt or protected derivative thereof. Macrophage proliferation has been implicated in a number of serious disorders, including AIDS (HIV)-associated dementia, AIDS-associated non-Hodgkin's lymphoma, and Alzheimer's disease. The invention also provides methods for aiding diagnosis and monitoring therapy of a macrophage-associated non-HIV associated dementia, especially Alzheimer's disease. The invention also provides methods of delaying development of macrophage-associated non-HIV associated dementias, including Alzheimer's disease, which entail administration of an agent which modulates macrophage proliferation.
CN102225192A Plaster for treating bone fracture and preparation method thereof The invention discloses a plaster for treating bone fracture and a preparation method thereof. The plaster comprises the following components in parts by weight: 15-30 parts of old ginger, 20-40 parts of cassia bark,10-20 parts of red paeony root, 20-30 parts of rhizoma arisaematis, 10-20 parts of radix angelicae, 20-40 parts of rehmannia root, 20-30 parts of rehmannia glutinosa, 30-50 parts of monkshood, 20-30 parts of peach kernel, 30-60 parts of safflower, 1-20 parts of Ligusticum wallichii, 20-40 parts of trogopterus dung, 30-50 parts of olibanum, 30-50 parts of myrrh, 30-60 parts of dragon's blood, 30-60 parts of pangolin, 20-40 parts of trigone, 20-30 parts of rhizome atractylyodis, 30-60 parts of rhizoma drynariae, 20-40 parts of native copper, 10-20 parts of musk and 30 parts of nux vomica. The plaster has the effects of tonifying liver and promoting bone, enhancing physique, promoting blood circulation and removing blood stasis and dredging collateral, is suitable for bone fractures such as light bone fraction, fracture and non-dislocation, blood stasis and the like, and has effects of promoting blood circulation and removing blood stasis, clearing heat and cooling blood, eliminating swelling and alleviating pain and setting a bone and regenerating a new bone.
CN101693011B Preparation method of magnetic medicine-carrying nano-particle The invention discloses a preparation method of magnetic carrying medicine nano-particles, which comprises the following characteristic steps of chemically coupling a medicine on the surface of magnetic nano-particles by amido bond to form the magnetic carrying medicine nano-particles; cladding silica layers on the surfaces of the magnetic carrying medicine nano-particles in a silica source hydrolysis mode to form nuclear shell compound nano-particles; then chemically modifying the surfaces of the nuclear shell type magnetic carrying medicine nano-particles with polyethylene glycol by adopting a reflux method, wherein the feeding mole ratio of the polyethylene glycol to the magnetic carrying medicine na no-particles is larger than 5:1; and finally, mechanically eroding thenuclear shell type magnetic carrying medicine nano-particles with polyethylene glycol through chemical modification by adopting inorganic alkali solution to from the magnetic carrying medicine nano-particles with multiple pore canals. The magnetic carrying medicine nano-particles prepared by the invention has the characteristics of strong particle chemical stability, uniform and controllable particle diameter, strong magnetic responsiveness, controllable medicine release action and remission of abrupt release phenomenon.
CN103585634A Docetaxel polymer nano-medicament preparation and preparation method thereof The invention discloses a docetaxel polymer nano-medicament preparation and a preparation method thereof. The preparation method comprises the following steps: (1) mixing a biodegradable polymer and a docetaxel original medicament, then dissolving the mixture in an organic solvent, mixing the organic solvent containing the polymer and the docetaxel with water and carrying out one-step synthesis to obtain nano-medicament particles; and (2) purifying and condensing the nano-medicament particles, filtering, sterilizing and carrying out freeze drying to obtain the docetaxel polymer nano-medicament preparation. According to the docetaxel polymer nano-medicament preparation and the preparation method thereof, the encapsulating efficiency, the particle size, the targeting property and the release property of the medicament can be optimized by adjusting the composition, concentration and the like of the polymer, and the controllability and nanoparticle uniformity of the nano-medicament are achieved. The docetaxel polymer nano-medicament preparation prepared by the preparation method disclosed by the invention is good in stability, has the characteristics of passive tumor targeting property, long circulation in vivo and the like, can be used for remarkably increasing the accumulation of the medicament in tumor cells and reducing the side effects of the medicament and has a favourable application prospect.
WO2011043371A1 Oxazole compound Disclosed is a novel and excellent prophylactic and/or therapeutic method for diseases associated with interleukin-1 receptor-associated kinase-4 (IRAK-4), which is based on an interleukin-1 receptor-associated kinase-4 (IRAK-4) inhibitory effect. Specifically disclosed is an oxazole carboxylic acid amide derivative which is characterized in that an oxazole that is substituted with a heteroaryl group at the 2-position is bonded to a heteroaryl ring via a carboxamide. The oxazole carboxylic acid amide derivative has a strong inhibitory effect on IRAK-4, and can serve as a prophylactic and/or therapeutic agent for diseases associated with IRAK-4 such as inflammatory diseases and autoimmune diseases.
US20110251242 Photostabilization of resveratrol with alkoxycrylene compounds The photostabilizing electronic excited state energy—particularly singlet state energy from resveratrol compounds—has been found to be readily transferred to (accepted by) α-cyanodiphenylacrylate compounds having an alkoxy radical in the four (para) position (hereinafter “alkoxycrylenes”) on one of the phenyl rings having the formula (I): wherein one of R1 and R2 is a straight or branched chain C1-C30 alkoxy radical, preferably C1-C8, more preferably methoxy, and the non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C30 alkyl radical, preferably C2-C20. The alkoxycrylene compounds of formula (I) significantly increase the photostability of resveratrol compounds in a composition by at least 3-fold and as much as 10-fold or greater. The ability of the alkoxycrylene compounds to stabilize the resveratrol compound is concentration dependent, with the amount of resveratrol photostabilization increasing with the concentration of the alkoxycrylene compound.
CN1884262A 4-amino piperidine compounds and their pharmaceutical use The invention relates to 4- amino piperidines compound showed in general formula 1, its optic antimer, racemic material, or its medicinal salt, and medical compound containing them. The invention also relates to the application in preparing drug preventing or treating pain after operation, cephalagra, visceralgia, neuralgia and addiction and survivability caused by analgesic such as opium drug.
US7700645 Comprising the ethanolate solvate of Prezista" aka darunavir ethanolate; improved pharmacokinetics;stability; bioavailability; purity; industrial scale; viricides New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed.
CN102908321A Albumin conjugated taxol nanoparticle freeze-dried preparation and preparation method thereof The invention discloses an albumin conjugated taxol nanoparticle freeze-dried preparation and a preparation method thereof. The preparation consists of the following components in percentage by weight: 0.1-2 percent of sterile taxol (nanoscale), 0.2-60 percent of human serum albumin (nanoscale), 0.2-60 percent of a surfactant, 0.2-30 percent of an oil phase, 0.2-60 percent of a freeze-dried framework agent, 0.1-5 percent of a pH regulating agent and 0.1-5 percent of a stabilizing agent. The invention provides an albumin conjugated taxol nanoparticle freeze-dried preparation, which can be used for enhancing the stability and safety of taxol, prolonging the medicament effect and enhancing the targeting capability. Albumin is taken as a carrier and an appropriate mixture ratio is selected, so that medicaments can be protected from being influenced by the environment, active ingredients are isolated, volatility and toxicity are lowered, an appropriate medicament releasing speed can be obtained, a slow and durable action is realized, and untoward effects are reduced.
CN101669954A Ferrous fumarate folic acid dispersible tablet and preparation method thereof The invention discloses a ferrous fumarate folic acid dispersible tablet and a preparation method thereof; the dispersible tablet is composed of 35-45 percent of composite of ferrous fumarate and folic acid and an acceptable carrier in pharmacy by mass percent; the mass ratio of ferric ions and folic acid in the composite of ferrous fumarate and folic acid is 150:1: the acceptable carrier in pharmacy comprises 30-60 percent of fillers, 2-10 percent of binding agents, 3-15 percent of disintegrants and 0.5-5 percent of lubricants by mass percent; the dispersible tablet is prepared by a wet granulation tabletting method and is rapidly disintegrated and evenly dispersed when meeting water, the effect is rapid, the bioavailability is high, and adverse reaction caused by overhigh local drug concentration of gastrointestinal tract can be alleviated or avoided, and the carrying and medicine taking are convenient; the preparation process is simple, the cost is low, the preparation is stable, safe and effective, thereby being suitable for industrial production.
EP1897552A1 Polymer-conjugated glycosylated neublastin The following class of molecule is disclosed: a dimer containing a first neublastin polypeptide and a second neublastin polypeptide, wherein: (a) at least one of the polypeptides is glycosylated; (b) at least one of the polypeptides is conjugated at its N-terminus to a water-soluble synthetic polymer; and (c) neither of the polypeptides is conjugated to a water-soluble synthetic polymer at a position other than the N-terminus. Such dimers possess the biological activity of wild-type neublastin while displaying enhanced serum half-life and enhanced potency relative to wild-type neublastin.
US20110177033 Ras responsive element binding protein 1 (rreb1) as a therapeutic target for thalassemias and sickle cell anemia A method of screening compounds capable of activating ζ and/or ε globin gene promoter activity in an erythroid cell is disclosed. The methods comprises contacting in a medium a compound to be screened with RREB1; wherein the medium comprises a polynucleotide comprising the nucleotide sequence of 5′-M-C-M-C-A-M-M-H-M-M-M-3′, wherein M is the nucleotide adenine or cytosine, and H is the nucleotide adenine, cytosine or thymine; the RREB1 bindable to the polynucleotide; determining binding of the compound to the RREB1; and determining change in binding of the RREB1 to the polynucleotide; wherein detection of binding of the compound to the RREB1 and change in binding of the RREB1 to the polynucleotide is indicative that the compound is capable of activating ζ and/or ε globin gene promoter activity. Also disclosed is a method of activating ζ and/or ε globin gene promoter activity in an erythroid cell.
US20120010246 Compositions and methods for treating diseases of the nail Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, which composition has a surface tension of 40 dynes/cm or less and has continuing spreadability, and which composition is effective in treating a disorder of the nail or nail bed.
US20100112088 Materials and methods for treatment of disorders associated with oxidative stress The subject invention pertains to materials and methods for the prevention and treatment of disease conditions associated with oxidative stress or a compromised reducing environment, including inflammatory bowel diseases such as Crohn's disease and ulcerative colitis. Therapeutic compositions of the invention include compositions that can neutralize hydrogen peroxide, such as reducing agents and oxidizing agents. In one embodiment, a therapeutic composition of the invention comprises a reducing agent such as sodium thiosulfate. Therapeutic compositions of the invention can optionally include compounds with antibacterial activity, compositions that inhibit bacterial adherence to cells and tissue, compositions that inhibits epithelial lipid peroxidation, compositions that add viscosity to a solution, compositions that inhibit most cells, and/or compositions that help to seal or repair tight junctions between cells of the colonic epithelium of the gastrointestinal tract. Methods of the invention include administration of compounds or compositions of the invention. In one embodiment, compounds or compositions of the invention are rectally instilled in a patient.
DE102004042021A1 Use of chitin, chitosan or their derivatives for prophylactic and therapeutic purposes in agricultural livestock production Chitin, chitosan or their derivatives are used for prophylactic and therapeutic purposes in agricultural livestock production. - ACTIVITY - Antibacterial; Antidiarrheic; Antiinflammatory. No biological data given. - MECHANISM OF ACTION - None given.
WO2010058846A1 4,6-diaminonicotinamide compound Disclosed is a 4,6-diaminonicotinamide compound which is useful as an active ingredient for a pharmaceutical composition, in particular, a pharmaceutical composition for treatment of diseases caused by undesirable and/or abnormal cytokine signaling. As a result of intensive studies on compounds having a JAK3 inhibitory effect, the inventors have found that the compound of the present invention, namely a 4,6-diaminonicotinamide compound has an excellent JAK3 inhibitory effect and is useful as an agent for prevention or treatment of diseases caused by undesirable and/or abnormal cytokine signaling.
CN1868464A Piduomode soft capsule and its prepn. method A pidotimod soft capsule is prepared from pidotimod and assistant chosen from diluent, cosolvent, solubilizer, suspending aid, and surfactant through proportional mixing, preparing soft capsule, solidifying by cooling in wind, drying, washing with proper solvent and drying.
US7071225 Arylaminopropane analogues and their use for the treatment of glaucoma Arylaminopropane analogues are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.
WO2013086425A1 The hydrobromide salt of pridopidine A salt of Pridopidine, a drug substance treats of Huntington's disease, include pharmaceutically acceptable hydfobromide salt, pharmaceutical compositions comprising this salt, and uses of this salt as a drug substance. The salt compounds improve symptoms of psychosis, including schizo-phrenia and schizophreniform disorders as well as drug induced psychotic disorders, behavioral disorders usually first diagnosed in infancy, childhood, or adolescence as well as in impulse control disorders, and speech disorders such as stuttering may improve. Other psychotic disorders not characterized as schizophrenia, schizo affective syndromes as well as psychotic symptoms, delusions and hallucinations induced by other drugs may also improve. Disruptive behavior disorders such as attention deficit hyperactivity disorder (ADHD), conduct disorder and oppositional defiant disorder may also improve, and tic disorders such as Gilles de la Tourette' s syndrome. Salt compounds may be used for treating substance abuse disorders as well as disorders characterized by misuse of food.
WO2005090330A1 N-piperidine derivates as ccr3 modulators Compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders and to pharmaceutical compositions containing them.
CN1923252A Oral medication for curing bone injury The invention discloses an oral powder preparation or capsules for treating orthopaedic diseases, wherein the raw mdddddaterials include (by weight ratio) hairy deer horn 3-4, sea dragon 3-4, Hippocampus japonicus 3-4, sea swallow 4-5, testiset penis phocae 4-5, musk 2-3, drynaria 5-6, eucommia bark 6-7, dragon's bone 3-4, Toricellia angulata 4-5, notoginseng 6-7, pangolin scales 3-4, dragon's blood resin 3-4, carpet bugle 6-7, frankincense 2-3, myrrh 3-4, native copper 5-6, achyranthes and cyathula root 3-4, saffron 5-6, ground beetle 5-6, dipsacus root 3-4, root of herbaceous peony 3-4, radix salvia miltiorrhiza 5-6, processed semen strychni 1-2, Flos Echinopsis latifolii 3-4, Bauhinia championii Benth. 3-4, Duyiwei 3-4 and licorice root 1-2.
WO2010084797A1 Hetero atom-containing compound Disclosed is a hetero atom-containing compound which has an excellent activity as an α2δ ligand. Specifically disclosed is a compound represented by general formula (I) or a pharmacologically acceptable salt thereof. (In the formula, R1 represents a hydrogen atom or the like; R2 represents a hydrogen atom or the like; R3 represents a hydrogen atom or the like; R4 represents a hydrogen atom or the like; R5 and R5' each represents a hydrogen atom or the like; R6 represents a hydrogen atom or the like; R7 represents a hydrogen atom, a C1-C6 alkyl group or a protecting group of carboxy group; and X, Y and Z may be the same or different and each represents a methylene group, an oxygen atom or a sulfur atom.)
US20080214496 Iron(III) polymaltose complex and iron(III)maltodextrin complex; improvements in immune defence and/or brain performance in patients who had a normal hematological result in respect of iron status The present invention relates to novel therapeutic uses of iron(III) complex compounds with carbohydrates or derivatives thereof, in the preparation of a medicament for improving immune defence and/or brain performance.
WO2005087230A1 Solid pharmaceutical preparation containing sparingly water-soluble drug Although bisacodyl has been coated with various coatings so as to be released in an area ranging from the lower part of the small intestine to the large intestine, it is less apt to sufficiently produce its effect because of its poor solubility. Furthermore, it has been necessary to incorporate the drug in a larger amount. No technique has been known in which bisacodyl and dioctylsodium sulfosuccinate are simultaneously released in an area ranging from the lower part of the small intestine to the large intestine. The solid pharmaceutical preparation is characterized in that a core particle comprising a sparingly water-soluble drug and dioctylsodium sulfosuccinate has been coated with an enteric coating so as to release the drug in an area ranging from the lower part of the small intestine to the large intestine. It can be an excellent medicine.
US7119111 2-oxo-1,3,4-trihydroquinazolinyl derivatives and methods of use Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
EP2638894A1 Pharmaceutical composition containing phospholipid Pharmaceutical composition comprises at least one systemically and/or locally acting topically applicable active substance and at least one phospholipid which improves the transport of the active substance through the cell membrane and contains phosphatidyl choline in a concentration of at least 60 wt.%, based on the phospholipid, where the composition has a liquid consistency that it is sprayable as droplets or as a foam. The composition has phospholipid comprising oil in a concentration of more than 7.5 wt.%. An independent claim is also included for use of at least one phospholipid as a permeation- and/or penetration accelerator in a pharmaceutical composition, where the composition has phospholipid comprising oil in a concentration of 7.5-2 wt.% in addition to phosphatidyl choline. ACTIVITY : Anesthetic; Antiallergic; Virucide; Neuroprotective; Cardiovascular-Gen; Fungicide; Analgesic; Anticonvulsant; Antiinflammatory; Antiandrogenic; Anticoagulant; Thrombolytic; Hemostatic; Antipruritic; Antidiabetic; Antimicrobial; Cerebroprotective; Immunosuppressive; Dermatological; Vulnerary; Neuroleptic; CNS-Gen; Muscle relaxant; Antiparkinsonian; Antiemetic; Antiparasitic; Antiasthmatic; Antitussive; Respiratory-Gen; Hepatotropic; Diuretic; Metabolic; Immunomodulator. No biological data given. MECHANISM OF ACTION : Leukotriene inhibitors; Opiate receptor antagonists; Platelet aggregation inhibitor; Histamine antagonist; Prostaglandin synthesis inhibitor; Calcium antagonist.
US20090239888 Methods for Inhibiting Amyloid Precursor Protein and Beta-Amyloid Production and Accumulation Compositions and uses of mGluR5 antagonists for the treatment and inhibition of amyloid precursor protein (APP), Aβ protein, and APP proteolytic products in Alzheimer's disease, Fragile X Syndrome, autism, and Down's Syndrome are provided. The invention provides methods for diagnosing Fragile X Syndrome via the assessment of Aβ1-42 levels in blood plasma.
US20140057897 Method of treating mixed lineage leukemia gene-rearranged acute lymphoblastic leukemias The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL.
US20110281856 Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates and methods of making said conjugates The present invention discloses a method for targeting maytansinoids to a selected cell population, the method comprising contacting a cell population or tissue suspected of containing the selected cell population with a cell-binding agent maytansinoid conjugate, wherein one or more maytansinoids is covalently linked to the cell-binding agent via a non-cleavable linker and the cell-binding agent binds to cells of the selected cell population.
WO2008089892A1 Phenothiazin derivates, method for the production thereof and use thereof as pharmaceuticals The invention relates to compounds of the formula (I), wherein the radicals R1, R2, R3, R4, R5, R6 and R7 and A and B are defined as indicated, and also to the physiologically tolerable salts thereof. The compounds are suited, for example, as anti-diabetics.
EP2448952A2 Novel guanosine-rich modified oligonucleotides and antiproliferative activity thereof The present invention relates to a novel modified oligonucleotide comprising at least one guanosine molecule and a modified nucleic acid with therapeutic efficacies. The present invention also relates to a pharmaceutical composition having cell apoptotic activity against cancer cells for preventing or treating cancer comprising a guanosine-rich modified oligonucleotide with at least one therapeutically effective modified nucleic acid (N), or its pharmaceutically acceptable salt as active ingredient.
US6838580 Opioid derivative 1. A peptide derivative represented by the following formula (1) or a salt thereof; wherein R1 is hydrogen atom or methyl group, R2 is hydrogen atom or hydroxy group and n is an integer of 1-8, provided that R1 is hydrogen atom when R2 is hydrogen atom, which has specific and high binding affinity with the μ-opioid receptor.
WO2014022427A1 Inhibition of rho and or rock and cell transplantation The present disclosure provides a multi-treatment combination to improve recovery after spinal cord injury or neurotrauma comprising: (a) Cell transplantation at the site of spinal cord injury and (b) Surgical delivery of BA-210. The combined treatment allows cells to be transplanted in the injury site during the acute trauma period, a time when the inflammatory response to neurotrauma adversely effects survival of transplanted cells. Early therapy delivered during critical care treatment after neurotrauma is essential for successful restorative therapy. The multi-treatment combination also provides a method to ensure that multi-potent transplanted cells do not become tumorigenic.
US7476662 Substituted tetracyclic imidazole derivatives, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-l-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-α]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof.
WO2007140662A1 Fluoroalkyloxy-containing combretastatin derivatives, preparation and use thereof Combretastatin derivatives of formula (I) , preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms , R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.
CN101036662A Medicament for treating beriberi and its preparation and medical bar The invention relates to a medicine for treating beriberi, a preparing method for the same and a medical rod. The medicine comprises compound ketoconazole ointment as a main material, and terramycin and vitamin B1 as accessories, with the preparing method of the medicine in such a way that: the terramycin and vitamin B1 are mixed according to a material formula and crushed into powder which are then added into the compound ketoconazole ointment, agitated, mixed uniformly to form the medicine for treating the beriberi. The medical rod of the invention includes a cotton rod, characterized that: a layer of medicine for treating the beriberi is coated on the cotton rod. The medicine formula of the invention is simple and has evident effect with high curative ratio for patient, low recurernce rate and simple preparing method; the medical rod with simple structure is convenient for using, can save the medicine, facilitates to treat the beriberi and is applicable to be popularized in a wide range.
US20120196933 Mexiletine prodrugs The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) pharmaceutical compositions containing such prodrugs. Methods for treating myotonic conditions, while reducing the inherent adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided.
CN103251615A Application of Aspeverin in preparation of medicines for treating laryngeal cancer The invention discloses an application of Aspeverin in preparation of medicines for treating laryngeal cancer, and belongs to the technical field of new medicinal applications. In vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) antitumor activity evaluation discovers that the Aspeverin also has an obvious inhibition function on the growth of human laryngeal cancer cell strains HET-2, TU686, M2E and M4E. Consequently, the Aspeverin can be used for preparing anti-laryngeal cancer medicines and has good development and application prospects. The application of Aspeverin in preparation of medicines for treating laryngeal cancer is disclosed for the first time, and the Aspeverin has an unexpected strong effect of inhibiting the laryngeal cancer cell activity.
EP1303305B1 Epoxy-steroidal aldosterone antagonist and calcium channel blocker combination therapy for treatment of congestive heart failure A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a calcium channel blocker is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred calcium channel blockers are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9α, 11α-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker verapamil HC1 (Benzenacetonitrile, (±)-α[3[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-3,4-dimethoxy-α-(1-methylethyl)hydrochloride) and the aldosterone receptor antagonist epoxymexrenone.
CN102846603A Preparation method for a compound antibiotic veterinary medicine The invention discloses a preparation method for a compound antibiotic veterinary medicine, wherein the medicine is composed of amoxicillin, clavulanate potassium and glucose. The medicine can be used to effectively treat all types of infections induced by penicillin-sensitive bacteria in poultry and livestock, has notable curative effect, is convenient to use, and is worth popularizing.
US20090253617 Diagnosis and treatment of attentional disorders This invention features methods and compositions useful for the treatment and diagnosis of attentional disorders including attention deficit hyperactivity disorder (ADHD). Also disclosed are methods for identifying compounds useful for such therapy.
CN102755306A Application of hydroxytyrosol in medicine used for preventing and curing obesity The invention relates to an application of hydroxytyrosol in a medicine used for preventing and curing obesity. The hydroxytyrosol is capable of effectively reducing the increment of weight, as well as accumulation of epididymis fat and perirenal fat during the generating process of obesity. Moreover, the hydroxy tyrosol can reduce the contents of triglyceride, free fatty acid and hunger insulinum in blood; and in addition, the hydroxy tyrosol is capable of obviously restraining the generation of fatty liver, reducing the weight of the liver, and restraining the accumulation of the triglyceride and cholesterol in the liver. Therefore, the hydroxy tyrosol has the function of promoting fat metabolism and cholesterol metabolism, can effectively protect the liver function, and cure and prevent the occurrence of obesity, and belongs to a drug with high curative effect, safety and simplicity.
CN102139051A Application of soft capsule capable of clearing heat and eliminating toxin in preparation of medicament for treating viral pneumonia The invention provides the application of a soft capsule capable of clearing heat and eliminating toxin in the preparation of a medicament for treating viral pneumonia, wherein the soft capsule capable of clearing heat and eliminating toxin comprises active components prepared from the following raw materials in parts by weight: 670 parts of gypsum, 134 parts of honeysuckle, 107 parts of figwort root, 80 parts of rehmannia root, 67 parts of forsythia, 67 parts of cape jasmine fruit, 67 parts of Chinese violet, 67 parts of baical skullcap root, 67 parts of Chinese gentian, 67 parts of indigowoad root, 54 parts of anemarrhena asphodeloides bunge and 54 parts of dwarf lilyturf tuber. Results of clinical tests of the soft capsule show that: when the soft capsule capable of clearing heat and eliminating toxin is adopted, pulmonary indexes can be reduced; and moreover, the soft capsule has an obvious inhibition effect on the mouse viral pneumonia caused by virus infection, and can be used for preparing the medicament for treating the viral pneumonia.
CA2260584C Androsterone derivatives for inhibiting dna binding of ap-1 and airway smooth muscle proliferation There is provided a method for the use of the adrenal steroid dehydroepiandrosterone and certain of its analogs to reduce growth of immortalized and malignant cell lines. Dehydroepiandrosterone and its potent analogs 16.alpha.-bromo-5-androsten-17-one, 16.beta.-bromo-5-androsten-17-one, 16.alpha.-fluoro-5-androsten-17-one, 16.beta.-fluoro-5-androsten-17-one, 16.alpha.-bromo-5-androstan-17-one, 16.beta.-bromo-5-androstan-17-one, 16.alpha.-fluoro-5-androstan-17-one, and 16.beta.-fluoro-5-androstan-17-one impair activation of secondary growth response genes and thus prove useful for treatment of asthmatic airway remodellina in man.
US20080102082 Policosanols and red yeast combined with astaxanthin and/or folic acid; antioxidant and antihypercholesterolemia activity Composition for oral administration, having a health-promoting effect on the cardiovascular system, comprising as active principles a policosanol or a mixture of policosanols, red yeast and an agent selected from astaxanthin and folic acid, preferably in combination with coenzyme Q10. The composition can be used in particular for the preparation of food supplements having health-promoting effects, such as eulipidaemic effect, correction of homocysteinaemia, antioxidant action and a protective effect on the vasal endothelium.
US20090143365 Derivatives of alkylpiperazine- and alkylhomopiperazine-carboxylates, preparation method thereof and use of same as fatty acid amido hydrolase enzyme inhibitors The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
US20090005344 Blocking inflammatory cytokines; tumor necrosis factor; phosphodieaterase inhibitor; antiarthritic agents; psoriasis; inflammatory bowel disorders; chronic obstructive pulmonary disorders Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.
US7253198 Hydroxyethylamine derivatives for the treatment of Alzheimer's disease The present invention relates to novel hydroxyethylamine compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
US7618961 A sulfonylamino-tetrahydro(1,3)thiazolo(5,4-c)pyridinyl or benzothiazole derivatives, for treating diabetes, syndrome X, obesity, glaucoma, hyperlipidemia, hyperglycemia, hyperinsulinemia, osteoporosis, tuberculosis, dementia The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
EP0861085B1 Anti-viral isolates obtained from leeches Methods, substances and compositions derived from leeches, bacteria associated with leeches, or combinations thereof are provided to prevent retroviral infections of host cells. More particularly, the invention relates to the inhibition of HIV replication. Thus the invention provides methods and substances for treating and/or preventing HIV infection and/or AIDS. The compounds or mixtures are obtainable by solvent extraction techniques and separation steps and were tested in the following manner. Two syncytium-forming HIV isolates, HIVAms55 and HIVAms37 were inoculated in PBMC and monocytes. During 14 days HIV induced cytopathic effects (CPE) (syncytium formation) and the virus production as determined by a p24 capture ELISA was monitored, after addition of leech head extracts. The result of these tests with the partly purified HIV inhibiting substance or substances is as follows: 3 fractions inhibited both syncytium formation and p24 antigen by 100 % at a concentration of: 0.067 mu M, 0.5 mu M and 0.17 mu M respectively in both HIV isolates. A fourth fraction underwent dilution series and inhibited both CPE and p-24 antigen 100 % from 0.5 mu M upwards in both HIV isolates.
CN102885083A Novel pesticide applied to multiple animals and plants The invention discloses a novel pesticide applied to multiple animals and plants. The pesticide is prepared from the following raw materials in part by weight: 5 to 8 parts of cosolvent, 2.5 to 5 parts of oxadiazon, 6 to 9 parts of n-butanol, 3.5 to 8.6 parts of sulfur, 0.8 to 2.5 parts of polyoxyethyl sulfonate, 4.5 to 6.7 parts of triethanolamine oleate, 3 to 5 parts of synergistic phosphorus, and 10 to 15 parts of water. The pesticide is low in animal toxicity, high in environmental compatibility, safe for the environment and effective for each living stage of mites, difficultly produces resistance, has a good mite and pest killing effect, and is easy to use, low in manufacturing cost and suitable for killing bacteria, mites and pests of multiple animals and plants.
CN103202811A Diflunisal solid dispersion and preparation method thereof The invention discloses a diflunisal solid dispersion and a preparation method thereof. The solid dispersion is composed of diflunisal as active components and high-polymer carrier materials. The high-polymer carrier materials are 40-90% of the diflunisal in total and selected from povidones, copovidones, and polyethylene glycol/vinyl caprolactam/vinyl acetate copolymer or hydroxypropyl methylcellulose. The preparation method adopts a hot-melting extrusion method. The diflunisal solid dispersion obtained is higher in solubility and quick and high in dissolving, bioavailability of indissolvable drugs is improved, drug dosage is reduced, and adverse drug reaction is reduced.
EP1368020B1 Method for identifying maxi-k channel blockers This invention relates to a method for identifying maxi-K channel blockers comprising using HEK-293 cells that have been stably transfected with both alpha and beta l subunits of the maxi-K channel and incubated with potassium channel blockers that selectively eliminate the endogenous conductances of the HEK-293 cells. Maxi-K channels are important for controlling a number of physiological processes. They play a role in the regulation of aqueous humor dynamics in the eye. Maxi-K channel blockers are known to reduce intraocular pressure.
CN1694874B Benzodiazepine derivatives and pharmaceutical compositions containing them Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: - R<1> represents C1-6 alkyl, aryl or heteroaryl; - R<2> represents hydrogen or C1-6 alkyl; - each R<3> is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, -CO2R , -CONR R, -NH-CO-R , -S(O)R , -S(O)2R , -NH-S(O)2R , -S(O)NR R or -S(O)2NRR wherein each R and R is the same or different and represents hydrogen or C1-6 alkyl; - n is from 0 to 3; R<4> represents hydrogen or C1-6 alkyl; - R<6> represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)-C(O)-, heteroaryl-C(O)-C(O)-, carbocyclyl-C(O)-C(O)-, heterocyclyl-C(O)-C(O)- or, -XR<6>; - X represents -CO-, -S(O)- or-S(0)2-; and - R<6> represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C 1-6hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C 1-6 hydroxyalkyl)-, aryl-(C 1-6alkyl)-O-, heteroaryl-(C 1-6alkyl)-O-, carbocyclyl-(C1-6 alkyl)-O-, heterocyclyl-(C1-6 alkyl)-O- or -NR R wherein each R and R is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl- (C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.
CN1927169A Norcantharidin magnetic nano microsphere and its preparing process The invention belongs to the field of composite materials and biomedical technology, specifically involves Norcantharidin-magnetic nanoparticles and their preparation methods. The invention take the biodegradable polymers as carriers, nanometer Fe304 as magnetic seeds, use hybrid emulsion -solvent volatilixation method (water-oil-water) to preparation packing parcels Norcantharidin magnetic nanoparticles. The main technological process includes the preparation, admixture and re- emulsification of two colostric fluid, solvent removal, removal of non-encapsulationed drug and free magnetic particles, magnetic microspheres washing cryodesiccation and so on. The Microspheres have smooth roundness surface, no adhesion, diameter below 400 nm, 6-9% Fe3O4 content, 8-15%drug encapsulation, and has a good biodegradable character. The magnetic microspheres have a broad prospect in experimental research and future clinical cancer therapy. The invention is characterized in simple process, good reproducibility, and low cost.
WO2014002967A1 4,6-hexadecadiene-2,4-dicarboxylic acid derivative Provided is a 4,6-hexadecadiene-2,4-dicarboxylic acid derivative or pharmaceutically acceptable salt thereof or the like, having anti-tumour activity and represented by general formula (I): [in the formula, R1 represents a hydroxy, –OR3 (in the formula, R3 represents a lower alkyl that may have a substituent, or an aliphatic heterocyclic group that may have a substituent) or –NR4R5 (in the formula, R4 and R5 are the same or different, and each represent a hydrogen atom, or a lower alkyl that may have a substituent), and R2 represents a hydroxy or –OR6 (in the formula, R6 represents a lower alkyl that may have a substituent or an aralkyl that may have a substituent)].
WO2005027929A1 Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and an estrogen The present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof a combination of a 2 alkylidene-1 9-nor-vitamin D derivative and an estrogen, or a pharmaceutically acceptable salt or prodrug thereof. Particularly, the present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof 2-methylene-19-nor-20(S)-1a,25-dihydroxyvitarjnin D3 and an estrogen, or a pharmaceutically acceptable salt or prodrug thereof.
CN101804196A Soybean-based whole protein type enteral nutrition powder and preparation method thereof The invention discloses a soybean-based whole protein type enteral nutrition powder. Every 100g of the product contains the following active ingredients: 14-19g of protein, 58-63g of carbohydrate, 16-22g of fat, 2-4g of compound vitamin and mineral substance and 0.6-1.2g of emulsifier; wherein the protein is mainly soybean protein isolate. The soybean based whole protein type enteral nutrition powder of the invention takes soybean protein as main protein source, a small quantity of casein is added, not only lactose is contained, but also the advantages of amimo acid in the two proteins are complemented, thus being more beneficial to digestion and absorption of human body. The invention also provides a preparation method of the soybean based whole protein type enteral nutrition powder.
US20110009332 Therapeutic Treatment Of Wounds The present disclosure relates to compositions and methods for treating wounded skin and/or increasing the mechanical strength of wounded skin through the administration of an effective amount of a proteasome inhibitor to such wounded skin.
CN102659787A Fluoro polyhydroxy pyrrole pyrrolizidine, and preparation method and application thereof The invention provides a fluoro iminosugar compound, and a preparation method and application thereof. The structure of the fluoro iminosugar compound is represented as formula (I) and formula (II), wherein n=1 or 2; X is hydroxyl or fluorine; R1, R2 and R3 are selected from hydrogen, hydroxyl, hydroxymethyl, benzyl, benzyloxy and benzyloxy methyl; R4 and R6 are selected from hydrogen, fluorine, methyl, monofluoro methyl, difluoro methyl, trifluoro methyl, hydroxymethyl, ethyl, ethoxyl, (1S)-hydroxyl ethoxyl, (1R)-hydroxyl hydroxyethyl, monofluoro hydroxyethyl to perfluoro hydroxyethyl, propyl, butyl or (monofluoro-substituted phenyl to perfluoro-substituted phenyl) or (monomethoxy-substituted phenyl to permethoxy-substituted phenyl); R5 is hydrogen, C1-C18 straight- or branched chain saturated alkane; R7 and R8 are hydrogen, fluorine, hydroxyl, methyl, ethyl, propyl, hydroxymethyl or trifluoromethyl. The preparation method of the fluoro iminosugar compound is simple and efficient. The fluoro iminosugar compound can serve as a potential medicine for restraining glycosidase or resisting tumors.
WO2008032777A1 Antibacterial peptide and use thereof Disclosed is an antibacterial peptide which occurs non-naturally and is artificially designed. The antibacterial peptide comprises a nuclear localization signal (NLS) sequence or a variant sequence thereof and a partial amino acid sequence derived from a leukemia inhibitory factor receptor (LIFR) or a variant sequence thereof.
CN102633719A Anilino-substituted-methylbenzofuryl quinoline derivatives, and preparation method and application thereof The invention discloses anilino-substituted-methylbenzofuryl quinoline derivatives, and a preparation method and application thereof. The chemical structure of the derivatives is disclosed as a general formula (I), wherein R1, R2, R3 and R4 are respectively H, F, Cl, Br, OH, OCH3, OC2H5, CF3, SCH3, C1-6 alkyl group, C3-6 cycloalkyl group, piperidyl group, morpholinyl group or piperazinyl group; R1, R2, R3 and R4 can be different or identical; R3 and R4 can respectively be ortho-position, meta-position or para-position of aniline; and X is C, NH, O or S. The anilino-substituted-methylbenzofuryl quinoline derivatives have obvious inhibiting action on multiple cancer cell strains and have small toxic action on normal cells; and therefore, the anilino-substituted-methylbenzofuryl quinoline derivatives can be used for preparing antineoplastic drugs, and have very high medical value and wide market prospects.
EP2178520A1 Drug formulations having inert sealed cores A drug composition comprising a coated bead is used in the manufacture of immediate release and/or controlled release drug compositions. In a specific embodiment, the bead includes an inert core of a water-soluble or water-swellable material, which has been coated with a seal layer formed from a non-polymeric hydrophobic material. The immediate and/or controlled release beads may be used to form tablets or capsules. A method of making the beads by sequential deposition of multiple layers on the inert cores is also described.
WO2011059416A1 Prophylactic antioxidant agent for protecting the tissues of an organism from the action of negative ecological factors or the consequences of smoking tobacco The invention relates to pharmacology, medicine, livestock breeding and poultry farming, and is directed towards producing agents and methods which can be used for prophylactic aims in order to reduce the risk of morbidity caused by negative ecology and by active or passive smokers breathing in tobacco smoke. The claimed prophylactic antioxidant agent contains sodium 2, 3-dimercaptopropane sulphonate and a pharmaceutically acceptable carrier. The agent effectively protects the tissues of an organism from the action of negative ecological factors or the consequences of smoking tobacco. Furthermore, the claimed agent can be used effectively in livestock breeding and poultry farming in order to increase productivity and reduce the death rate of animals and birds.
CN1985988B Novel medicine composition for treating hepatic diseases The present invention belongs to the field of medicine technology, and is especially a kind of medicine composition and its preparation process. The medicine composition is prepared with kurarinone 4-400 weight portions, glutathione 3-300 weight portions, and tiopronin 1-100 weight portions. The medicine composition may be prepared into different pharmaceutically acceptable forms, preferably injection and oral preparation. It has the pharmacological activities of antagonizing virus, improving liver cell function, antagonizing liver fibrosis, regulating immunity, diminishing inflammation, etc.and may be used in treating various hepatic diseases, viral hepatosis, medicinal hepatosis, alcoholic hepatosis, etc.
WO2010068918A2 Novel targets for treatment of hypercholesterolemia In certain embodiments this invention this invention pertains to the discovery that inhibition of myosin light chain interacting protein (Mylip) can mitigate one or more symptoms of hypercholesterolemia. Methods of treating hypercholesterolemia and methods of screening for agents to treat hypercholesterolemia are provided.
WO2010073825A1 Antibacterial composition and antiviral composition each containing silicon-containing compound, antibacterializing method, cleaning/mouth cleaning method, and method for immobilizing antibacterial agent or antiviral agent Disclosed is an antibacterial composition which is highly safe and has excellent antibacterial properties, by using a silicon-containing compound that is obtained by a specific manufacturing method. The antibacterial composition has a more stable antibacterial component, and is capable of providing teeth with antibacterial properties, while being also capable of cleaning an object or the mouth. Also disclosed are: an antiviral composition which is highly safe and has excellent virus deactivation ability; an antibacterializing method, a cleaning method and a mouth cleaning method, each using the antibacterial composition or the antiviral composition; and a method for immobilizing an antibacterial agent or an antiviral agent. The antibacterial composition is characterized by containing a silicon-containing compound which is represented by general formula (1) and obtained by reacting a specific triethoxysilyl compound in an ethanol solvent.
US6884800 Nitrogen compounds such as 10-Chloro-3-imidazol-1-yl-2,3-dihydro-1H-pyrido(3,2,1-kl)phenothiazine, used for prophylaxis of respiratory system and skin disorders, autoimune diseases, tumors or atherosclerosis and AIDS Imidazole compounds of the formula I in which R1 and R2, independently of one another, each denote A1, OA1, SA1 or Hal, A1 denotes H, A, alkenyl, cycloalkyl or alkylenecycloalkyl, A denotes alkyl having 1-10 carbon atoms, Hal denotes F, Cl, Br or I, and X denotes O, S, SO or SO2, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors, and their use for the preparation of a medicament.
US20100267839 Diarylalkanes as potent inhibitors of binuclear enzymes The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.
US20100273884 Method for stable and controlled delivery of (-)-hydroxycitric acid The present invention provides stable encapsulated (−)-hydroxycitric acid (“HCA”)-containing compositions and methods of making the same. A method is provided by which the hygroscopic salts of HCA in their relatively pure and active forms, including especially the potassium salt, but also including the sodium salt, are rendered non-hygroscopic and stable (that is, not prone to lactonization, not readily subject to attachment to ligands which inhibit absorption or lead to excretion, and so forth) such that these HCA salts might be included in dry delivery formats, liquid delivery and in controlled-release vehicles. The nonhygroscopic salts of HCA and its derivatives likewise may be protected against acid degradation, lactonization and undesirable ligand binding when exposed to acidic environments or other challenging conditions. The method taught herein can be employed to reduce the polar/ionic qualities of HCA salts and derivatives when presented to the intestinal lumen to provide advantages in absorption.
US20080280996 Rheumatic diseases; antiarthritic agents; osteoarthritis; lupus; inflammatory bowel disorders; psoriasis; atherosclerosis; cyclooxygenase inhibitor; antidepressants; blocks production of cytokines, tumor necrosis factor, prostaglandins The invention concerns the use of caryophyllenes related to medicaments and to the treatment of bodily conditions of inflammation and inflammatory pain.
EP2668169A1 Tetrazole compounds and methods of making and using same Described herein are tetrazole compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tetrazole compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
CN103570685A Salt of 6,7-dimethoxyquinoline derivative The invention relates to N-(4-(6,7-dimethoxyquinoline-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidinone-1-carboxamide and a fumarate of a derivative thereof or a pharmaceutically acceptable solvate and an application thereof in preparation of medicaments for treating cancers.
US20120052061 Therapies for treating cancer using combinations of cox-2 inhibitors and anti-her2(erbb2) antibodies or combinations of cox-2 inhibitors and her2(erbb2) receptor tyrosine kinase inhibitors Described herein are compositions and methods for using these compositions in the treatment of cancer, tumors, and tumor-related disorders in a subject.
US8741935 Nicotine delivery product and method for producing it A nicotine delivery product comprising the reaction product of a nicotine/cation exchange resin complex and an organic polyol; and a method for preparing it comprising (a) mixing an aqueous suspension of a nicotine/cation exchange resin complex with an organic polyol or an aqueous solution thereof, and (b) removing water from the mixture to produce said nicotine delivery product. The nicotine delivery product has a nicotine release rate of at least 80% over a 10 minute period. It is particularly suited for use in smoking substitution devices delivering nicotine such as chewing gum, patches, lozenges, melting tablets and tablets for chewing.
CA2579923A1 Anti-parasitic and/or anti-viral and/or anti-microbial compositions Voacamine and its natural and synthetic derivatives such as 16'~decarbometheoxyvoacamine, N6-demethylvoacamine, voacamidine, tabernamine, ervahamine A, vobasine and coronaridine are useful as anti-microbial, anti-parasitic and anti-viral agents. A basic extract of the tertiary alkaloids present in plants of the genus Peschiera or Voacanga, expecially Peschiera fuchsiaefolia can be isolated and used directly as such an agent.
EP1597259B1 Nitrogen-substituted hexahydropyrazino 1,2-a pyrimidine-4,7-dione derivatives, method for the production and use thereof as medicaments The invention relates to nitrogen-substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, in addition to the physiologically compatible salts thereof and physiologically functional derivatives. The invention also relates to compounds of formula (I), wherein the radicals have the cited meanings, the physiologically compatible salts thereof and methods for the production thereof. Said compounds can be used, for example, as anorectics.
EP1715855A2 Anti-viral therapeutics Heterocyclic compounds of formula (I), (II), (III), and (IV) and methods of treating or preventing an HIV-mediated disorder by administering a compound of formula (I), (II), (III), or (IV) are described herein.
US20090275499 Nonstructural protein ns1 as a novel therapeutic target against flaviviruses The secretion or biological activity of Flaviviruses, as well as the biological activity of NS1 protein from Flavivirus-infected cells, can be inhibited by contacting the cells or the protein with cholesterol inhibitors, sphingolipid inhibitors, glycosphingolipid inhibitors, or molecules comprising an amphipathic, amphiphilic, or hydrophobic region which interacts with NS1 protein.
WO2012027712A3 Potent and selective inhibitors of hepatitis c virus The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.
US7105540 Cholinesterase inhibitors to treat disorders of attention The present invention provides novel methods of treating disorders of attention or improving attention in humans by administering an effective amount of a cholinesterase inhibitor.
US7026476 Intermediate arylamine compounds Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.
US20100062992 Salts of 5-Azacytidine The present invention relates to salts of 5-azacytidine as well as methods for synthesizing the salts described herein. Pharmaceutical compositions and methods of using the 5-azacytidine salts are also provided, including methods of administering the salts or pharmaceutical compositions thereof to treat conditions, such as cancer and hematological disorders.
US7776865 checkpoint kinase inhibitors; for treating and preventing proliferative diseases such as cancer, inflammation and arthritis, neurodegenerative diseases such Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases In its many embodiments, the present invention provides a novel class of amino-substituted pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. An illustrative compound is shown below:
WO2004108141A3 Bach-o-protein coupled receptor releated methods We disclose that ADP is capable of binding to and activating the BACH-Gprotein coupled receptor (BACCH-GPCR). We describe methods of identifying a compound or an agent which is capable of modulating the ability of ADP to activate the BACK-GPCR. We also describe using ADP or derivatives thereof or modulators of the binding between ADP and the BACK-GPCR for treating diseases associated with BACH-GPCR consisting of trigeminal neuralgia, pain of various origins, irritable bowel syndrome, bladder instability, Barrett’s esophagus, glaucoma, pain associated with cancer, diabetic neuropathies, Herpes virus infections, migraine and skin sensitivity associated with migraine, allodynia, toothache, neuroma, dementia, dyslexia, dyskinesias, tremor, Parkinson’s, benign essential tremor, chorea, epilepsy or ballismus, for example occurring through stroke, trauma, degeneration and malignancy, chronic pain (peripheral or visceral) and relapsing remitting pain such as migraine, dry eye disorder, cyctic fibrosis, hyperactive bladder, hypercholesterolaemia, dislipdaemias and obesity.
CN101899059A Pyrrolidine-containing dicyclic cephalosporin derivatives The invention belongs to the technical field of medicine, in particular to pyrrolidine-containing dicyclic cephalosporin derivatives shown as the general formula (I) and pharmaceutically acceptable salts thereof, wherein the meanings of R1, R2, R3, R4, R5, X, Y, m, n and P are defined in the specification. In addition, the invention also provides a preparation method of the compounds, a medicine composition containing the compounds and application of the compounds in preparing medicaments for treating and/or preventing infectious diseases.
WO2011050030A1 Alpha adrenergic receptor modulators Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor, in particular the alpha 2C receptor. The compounds can include N-(2,3-substituted phenyl)-3,4-dihydro-2Hpyrrol-5-amine derivatives. Methods of making, using and formulating these compounds are described
US20090170813 Hypophosphorous Acid Derivatives and their Therapeutical Applications Hypophosphorous acid derivatives having Formula (I) wherein .M is a [C(R3,R4)]n1-C(E,COOR1,N(H,Z)) group, or an optionally substituted Ar—CH(COOR1,N(H,Z)) group, or an a, β, or a β, g-cyclic amino acid; .R1 is H or R, R being an hydroxy or a carboxy protecting group; .Z is H or an amino protecting group R′, benzyl oxycarbonyl, benzyl or benzyl substituted; .E is H or a C1-C3 alkyl, aryl, an hydrophobic group; .R2 is selected in the group comprising: D-CH(R6)—C—(R7,R8), (R11,R12)CH—C(R9,R10), D-CH(OH), D-[C(R13,R14)]n3—, C[(R15,R16,R17)]n4, D-CH2, (R18)CH═C(R19), D-(M1)n6—CO, Formula (II), PO(OH)2—CH2 or (PO(OH)2—CH2), (COOH—CH2)—CH2, with -D=H, OH, OR, (CH2)n2OH, (CH2)n1OR, COOH, COOR, (CH2)n2COOH, (CH2)n1COOR, SR, S(OR), SO2R, NO2, heteroaryl, C1-C3 alkyl, cycloalkyl, heterocycloalkyl, (CH2)n2-alkyl, (COOH,NH2)—(CH2)u1-cyclopropyl-(CH2)u2—, CO—NH-alkyl, Ar, (CH2)n2—Ar, CO—NH—Ar; —R3 to R19 being H, OH, OR, (CH2)n2OH, (CH2)n1OR, COOH, COOR, (CH2)n2COOH, (CH2)n1COOR, C1-C3 alkyl, cycloalkyl, (CH2)n1-alkyl, aryl, (CH2)n1-aryl, halogen, CF3, SO3H, (CH2)xPO3H2, with x=0, 1 or 2, B(OH)2, Formula (III), NO2, SO2NH2, SO2NHR; SR, S(O)R, SO2R, benzyl; -M1 is an alkylene or arylene group; -n1=1, 2 or 3, n2=1, 2 or 3, n3=0, 1, 2 or 3 and n4=1, 2 or 3, n5=1, 2 or 3, n6=0 or 1, u1 and u2, identical or different=0, 1 or 2, with the proviso that Formula (I) does not represent the racemic (3R,S) and the enantiomeric form (3R) of 3 amino,3-carboxy-propyl-2′-carboxy-ethylphosphinic acid; 3 amino,3-carboxy-propyl-4′carboxy,2′carboxy-butanoylphosphinic acid; 3 amino,3-carboxy-propyl-2′carboxy-butanoylphosphinic acid; 3 amino,3-carboxy-propyl-3′amino, 3′carboxy-propylylphosphinic acid; and 3 amino,3-carboxypropyl-7′amino-2′, 7′-dicarboxyheptylphosphinic acid, said hypophosphorous acid derivatives being diasteroisomers or enantiomers. Application as drugs.
CN101032476A Medical combination including rhein or diacetylrhein and the preparing method thereof The present invention relates to one kind of medicine composition containing rheinic acid or diacetyl rheinic acid and its pharmaceutically acceptable salt, dispersant carrier material and other supplementary material. The medicine composition is prepared through a melting process, a solvent process, a melting-solvent process or a fine grinding process to prepare effective component dispersoid; and further dropping the dispersoid into condensing agent to prepare dripping pill, or other steps to prepare different other preparations. The medicine composition of the present invention has raised bioavailability, and may be applied widely in treating osteoarthritis, rheumatoid arthritis, hyperlipemia and other diseases.
WO2014048881A1 Combination of regorafenib and acetylsalicylic acid for treating cancer The present invention relates to pharmaceutical compositions and combinations comprising regorafenib and acetylsalicylic acid, or a hydrate, solvate, metabolite or pharmaceutically acceptable salt thereof or a polymorph thereof for treating, preventing or managing diseases and conditions including hyperproliverative disorders such as cancer in humans and other mammals.
US8147872 Pharmaceutical compositions of drugs and neutralized acidic polymers Pharmaceutical compositions comprised of low-solubility and/or acid-sensitive drugs and neutralized acidic polymers are disclosed.
CN103113384A Catechin derivative named Fuzhuansu B, and preparation method and application thereof The invention belongs to the technical field of chemistry, and particularly relates to a catechin derivative named Fuzhuansu B, and a preparation method and application thereof. The invention firstly provides a catechin derivative named Fuzhuansu B separated from Fuzhuan brick tea. The preparation method comprises the following steps: taking the Fuzhuan brick tea, and pulverizing the Fuzhuan brick tea; extracting the pulverized Fuzhuan brick tea with an organic solvent, and concentrating the extracting solution under reduced pressure to obtain a paste extract; and separating and purifying the paste extract to obtain the Fuzhuansu B. The invention also provides application of the catechin derivative named Fuzhuansu B in preparing anti-cervical carcinoma (HeLa) medicines. The invention provides a catechin derivative with bioactivity, has important meanings for the fields of agriculture and medicine, and also provides wide prospects for effectively developing and utilizing Fuzhuan brick tea. The preparation method provided by the invention is simple, and low in cost.
WO2014161918A1 Therapeutic uses of empagliflozin The present invention relates to certain SGLT-2 inhibitors for treating and/or preventing oxidative stress, for example in patients with type 1or type 2 diabetes, as well as to the use of such SGLT-2 inhibitors in treatment and/or prevention of cardiovascular diseases in patients, for example type 1or type 2 diabetes patients. The present invention further relates to certain SGLT-2 inhibitors for treating and/or preventing a metabolic disorder and preventing, reducing the risk of or delaying the occurrence of a cardiovascular event in patients, for example patients with type 1 or type 2 diabetes.
US20070265249 Fused Bicyclic Aromatic Compounds that are Useful in Treating Sexual Dysfunction The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein A, L, D and B1 are as described in the specification.
CN1919268A Mouth-wash medicine for treating stomatocace and preparation method thereof Disclosed is a mouth-washing gargle for treating ulcerative stomatitis and its preparation, wherein the medicament is prepared from the following raw materials (by weight portion): yellow corktree bark 25-30g, honeysuckle flower 18-20g, mentha, licorice root each 8-10g, borneol 4-6g. The invention realizes easy material availability, simplified preparation, low cost, and quick effect.
CN103006743A Scald agent production method The invention relates to a scald agent production method, and belongs to the field of drug production, wherein disadvantages of not significant treatment effect and long treatment time of the generally scald drugs can be effectively solved with the scald agent. The production method comprises: placing 8 g of borneol in a grinding machine to grind the borneol into fine powder, and filling the grinded borneol fine powder into a drug-loaded cylinder to be spare; placing 20 g of camphor into the grinding machine to grind into fine powder, and filling the grinded camphor fine powder into another drug-loaded cylinder to be spare; taking a clean drug-loaded cylinder, adding 200 ml of a calcium hydroxide solution (0.3%), then adding 1.2 g of olive oil, uniformly stirring with a wood rod, and then slowly adding 20 g of the camphor powder, wherein continuous stirring with the wood rod is performed during adding; adding 8 g of the borneol powder to the cylinder, stirring for 10 min with the wood rod so as to uniformly mix the raw materials; and packaging with a plastic bottle, wherein each plastic bottle is packaged with 150 ml of the obtained solution. The production method is mainly used for scald agent production.
US20090060905 Use of 15-Lipoxygenase Inhibitors for Treating Obesity The invention concerns the treatment of obesity, in particular abdominal visceral obesity. More specifically, the invention concerns the use of selective 15-lipoxygenase (LO) inhibitors for preparing medicines useful in the treatment of obesity, or at least abdominal visceral obesity, and/or its consequences.
US20110212961 Pyrazole Derivatives as Kinase Inhibitors The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: wherein X is a six-member ring selected from phenyl, pyridine, or pyrimidine; Y is H, an alkenyl, a substituted alkenyl, or alkynyl, and R is H or alkyl. Pharmaceutical compositions for treating various disorders such as cancers, the compositions including compound I are also provided.
EP2265589A1 Arylsulfonyl pyrazoline carboxamidine derivatives as 5-ht6 antagonists This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5- HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.
CN101795692A Therapeutic substituted cyclopentanes for reducing intraocular pressure Disclosed herein are compounds having formula (I) wherein a dashed line represents the presence or absence of a bond; Y is an organic acid functional group, or an amide or ester thereof; or Y is hydroxymethyl or an ether thereof; or Y is a tetrazolyl functional group; A is -(CH2)6-, cis -CH2CH=CH-(CH2)3-, or -CH2C=C-(CH2)3-, wherein 1 or 2 carbon atoms may be replaced by S or O; or A is -(CH2)m-Ar-(CH2)o- wherein Ar is interarylene or heterointerarylene, the sum of m and o is 1, 2, 3, or 4, and wherein 1 -CH2- may be replaced by S or O, and 1 -CH2-CH2- may be replaced by -CH=CH- or -C=C-; U1 and U2 are independently selected from -H, =O, -OH, -F, -Cl, and -CN; and B is aryl or heteroaryl, for use as acular hypotensive agent.
WO2014143659A1 Irreversible covalent inhibitors of the gtpase k-ras g12c Irreversible inhibitors of K-Ras, H-Ras or N-ras protein comprising a G12C mutation are provided. Also disclosed are methods to regulate the activity of K-Ras, H-Ras or N-ras protein comprising G12C mutation and methods to disease mediated by K-Ras, H-Ras or N-ras G12C.
CN101503445A Nucleic acid molecule SI-CYPJ-32 and use thereof in anti-cancer medicine preparation The invention belongs to the biological medicine field, relating to nucleotide molecules and the application thereof in the preparation of antitumor medicines. The invention provides the nucleotide molecules for preparing the antitumor medicines. The nucleotide molecules have the activity for inhibiting the tumor growth and the sequence thereof comprises 5'-CCUUUCCAAAUACGGUGUA-3' or 5'-CCTTTCCAAATACGGTGTA-3' which is known as SI-CYPJ-32 in the invention. The nucleotide molecules SI-CYPJ-32 can obviously inhibit the tumor cell proliferation; when the nucleotide molecules are applied to a naked mouse, the tumor body growth of the naked mouse is obviously inhibited compared with the control naked mouse in the same condition of culture, and the phenomenon becomes obvious day by day as time goes on. The invention provides a new approach and means for the tumor treatment and mitigation.
US7662977 Such as 2-cationic amino-4-oxo-chromene derivatives; water solubility, pharmacokinetics; reduced side effects; anticancer agents The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.
EP2416761A1 Desfesoterodine in the form of a tartaric acid salt The invention relates to desfesoterodine in the form of a tartaric acid salt, in particular in the polymorphic "form R", and to a process for the production thereof. In a second aspect, the invention relates to the desfesoterodine according to the invention in micro-encapsulated form.
CN101703517A Tinidazole/miconazole nitrate/neomycin self-microemulsion soft capsules for vagina and preparation method thereof The invention belongs to the field of medicinal preparations, and relates to self-microemulsion soft capsules containing tinidazole/miconazole nitrate/neomycin for vagina and a preparation method thereof. The self-microemulsion soft capsules for the vagina consist of tinidazole, miconazole nitrate and neomycin sulfate in treatment effective dose, and can be used for multiple vaginitis. The methodfor preparing the self-microemulsion soft capsules comprises the following steps: heating surfactant, co-surfactant and oil phase to melt, adding the tinidazole, the miconazole nitrate and the neomycin sulfate in prescription amount into the melted mixture, and stirring the mixture till dissolving to obtain the self-microemulsion soft capsules. The self-microemulsion soft capsules prepared by themethod improve the bioavailability of the medicament in vivo, have quick response, and overcome the defect that the common vaginal tablets have lower bioavailability; and meanwhile, serving as a new composite dosage form, the formulation is scientific and novel and can provide a newer and better dosage form selection for both doctors and patients. The preparation process is simple and has no special requirement on preparation environment, the cost is low, the product quality is stable, and the preparation method is suitable for industrialized production.
EP1768602A4 Combination drug therapy for reducing scar tissue formation The present invention describes various devices and methods wherein a cytostatic antiproliferative drug, either alone or in combination with other drugs, is placed between internal body tissues to prevent the formation of scar tissue and/or adhesions during healing of a wound or surgical site. Specific devices to achieve this administration include, but are not limited to, a permanent implant or a biodegradable material having an attached antiproliferative drug such as sirolimus. These antiproliferative drugs may be combined with other drugs including, but not limited to, antiplatelets, antithrombotics or anticoagulants. The present invention also contemplates methods to a reduce scar tissue and/or adhesions or adhesion formation at an anastomosis site. In particular, a cytostatic antiproliferative drug is administered to an arteriovenous shunt anastomoses in patients having end-stage renal disease.
CN102743364A Application of metformin in preparations of drugs for treatment of Parkinson's disease The present invention provides an application of metformin in preparations of drugs for treatment of Parkinson's disease (PD). Experiment results show that: with the metformin, behavioral disorders of PD model mice are significantly improved; dopaminergic neuron loss of mice midbrain substantia nigra compact part (SNc) and ventral tegmental area (VTA) due to MPTP/p is reduced; levels of dopamine (DA) and metabolites thereof in corpus striatum are improved; excessive proliferation activation of astrocyte is inhibited; and reduction of dopaminergic neuron cell line SH-SY5Y cell viability, and increases of lactate dehydrogenase (LDH) generation and reactive oxygen species (ROS) generation are inhibited, wherein the reason of the reduction of dopaminergic neuron cell line SH-SY5Y cell viability, and the increases of lactate dehydrogenase (LDH) generation and reactive oxygen species (ROS) generation is MPP<+>. In addition, the results show that the metformin provides pharmacological effects for treatment of PD. According to the application of the present invention, the metformin is adopted as an active ingredient to prepare drugs for treatment of PD.
CN102764262A Application of oleanolic acid and retinoic acid pharmaceutical composition to medicament for treating insulin resistance and diabetes The invention discloses application of an oleanolic acid and retinoic acid pharmaceutical composition to medicament for treating insulin resistance and diabetes. Intraperitoneal injection of the oleanolic acid and retinoic acid pharmaceutical composition to diabetic animal can significantly lower the blood glucose level; and addition of the oleanolic acid and retinoic acid pharmaceutical composition in culture solution for culturing liver cells can significantly promote transmission of an insulin signal. Therefore, the oleanolic acid and retinoic acid pharmaceutical composition can be applied to medicaments for treating diabetes, insulin resistance and metabolic syndrome closely related to insulin resistance.
CA2843431A1 Sandalwood oil and its uses related to skin disorders Provided herein are compositions of sandalwood heartwood oil and methods of making and using such compositions.
CN102218043A LDH (Layered Double Hydroxides) supermolecular assembly type aspirin sustained release tablet and preparation method thereof The invention relates to an LDH (Layered Double Hydroxides) supermolecular assembly type aspirin sustained release tablet, wherein three levels of supermolecules consisting of dextran, layered double hydroxides and aspirin are used as a medicine barrier, hydroxypropyl methylcellulose is used as a material of a gel skeleton, and the sustained release tablet is prepared by carrying out direct tablet compressing on powder. Auxiliary materials adopted by the LDH supermolecular assembly type aspirin sustained release tablet are good in liquidity, the sustained release tablet can be prepared by carrying out direct tablet compressing on the powder, the process is simple and fast and the cost is low; DET (Dextran)-LDH (Layered Double Hydroxides)-ASP (Aspirin) three-level supermolecule assembly isadopted to overcome the defects of acid dissolution and easiness in sudden release of LDH-ASP so that the system biocompatibility is improved, and by cooperative control of HPMC (Hydroxypropyl Methylcellulose)-DET-LDH, the sustained release performance is obviously improved; and compared with traditional aspirin sustained release tablets with organic auxiliary materials, the LDH supermolecular assembly type sustained release tablet has special cytobiology advantages, relatively high bioavailability, obvious releasing effect and specially sustained transferring and releasing process.
CN102786483A Medicinal use of 4-(4-phenylpiperazino)quinazoline derivatives The invention belongs to the field of biological pharmacy, relates to a medicinal use of 4-(4-phenylpiperazino)quinazoline derivatives and especially relates to a use of the 4-(4-phenylpiperazino)quinazoline derivatives in preparation of drugs for treating nervous system diseases and especially in preparation of dopamine D3 receptor inhibitors. A result of a biological activity test shows that the 4-(4-phenylpiperazino)quinazoline derivatives have good effects of inhibiting D3 receptors. The 4-(4-phenylpiperazino)quinazoline derivatives can be used as drug lead compounds, be synthesized into dopamine D3 receptor inhibitors, and be further used for preparation of drugs for treating schizophrenia and Parkinsonism caused by dopamine system dysfunction.
DE102004026026A1 New 2-(hetero)aryl-tetrahydroquinoline derivatives and 1,2,3,4-tetrahydro-1,5-naphthyridine derivatives are mitotic motor protein Eg5 inhibitors used as anticancer agents for treating carcinoma or leukemia 2-(Hetero)aryl-substituted 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydro-1,5-naphthyridine derivatives (I) (including tricyclic analogs, e.g. pyrano-quinolines), are new. 2-(Hetero)aryl-substituted 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydro-1,5-naphthyridine derivatives of formula (I) and their derivatives, solvates, tautomers, salts and stereoisomers (including mixtures in all proportions) are new. W = CH or N; R1> - R3> = H, R, A, Ar, halo, (CY2)n-Q1>, cycloalkyl, SMe, SCN, CF3, OCF3, OA, SCF3, SF5, SiMe3, CO-(CY2)n-Me, CH(CH2)n-Q2>, NCO, NCOOR, N(CH2)nOH, CHNH2, C(OH)R, CHNCOR, N(CH2)nCOOR, N(CH2)nCONR2, XCONR(CH2)nNR2, N((CH2)nXCOOR)-CO(CH2)nAr, N((CH2)nXR)-Q3>, N((CH2)nNRCOOR)CO(CH2)nAr, N((CH2)nNR2)-Q4>, O(CH2)nNR2, X(CH2)nNR2 or NCO(CH2)nNR2, or R1> + R2> = -N-C(CF3)=N-, -N-CR=N- or -N-N=N-; Q1> = SA, SCF3, SCN, CF3, OCF3, OH, COOR, CN, halo, NR2, OA, OCOA, CONR2, NHCOA, NHSO2A or N-pyrrolidone; Q2> = NRCOOR, COOR, OH, NR2, Ar, R1> or X(CH2)nAr; Q3> = CO(CH2)nAr, CO(CH2)nXAr or SO2(CH2)nAr; Q4> = CO(CH2)nAr, CO(CH2)nNRAr or SO2(CH2)nAr; Ar = aryl or heteroaryl; Y = H, A or halo; A = alkyl or cycloalkyl (both os by one or more halo); R = H or A, or geminal groups R = (CH2)5, (CH2)4, (CH2)2X(CH2)2 or (CH2)2Z(CH2)2; (MK#12) R4>, R5> = H, N-pyrrolidone residue (optionally substituted by one or more of OR, NO2, halo, CF3, OCF3, CN, NR2, SR or Ar), -X(CH2)2OR, -XCO(CH2)nMe, -X(CH2)2NR2, R1>, arylthio, aryloxy or CH2SiMe3, or R4> + R5> = X(CR2)2, X(CR2)3, X(CHCH2OR)(CH2)2, X(CHCH2NR2)(CH2)2, X(CH2)2NR2, (CR2)3, X(CR2)4, CR=CR-CR=CR, XCHQ(CR2)2, XCHQCR2, R-N-(C=X)-N-R or XC((CH2)nOR)2CH2CH2; X = O, S or NR; Q = halomethyl, CHO, CORa>, CH2Ra>, CH2OCORa>, CH2NCOR1>, CH2N(R1>)2, CH2OR1>, CH2OCON(R1>)2, CH2OCOOR1>, CH2NHCON(R1>)2 or -CH2NHCOOR1>; Ra> = -(CH2)n-(X(CH2)n)m-Q5>, 4-(CH2CH(CONH2)-COO-(CH2)nQ6>)-1H-im idazol-1-yl, 2-oxa-3-oxo-4,7,7-tri-(R)-bicyclo-(2,2,1)-heptan-ylcarbo nyloxy, OR, NHR2, NR2, NR(CH2)n-aryl, NR(CH2)n-OR, COOR, N-pyrrolidone, OCOR, NR(CH2)n-NR2, N((CH2)nNR2)CO(CH2)nQ7>, N((CH2)nNHCOOR)-CO-aryl, R1>, N(CH2(CH2)nOR)2, NR(CH2)nNCOOR, X(CH2)nX(CH2)nXR, X(CH2)nX(CH2)nOH, NR(CH2)nO(CH2)nOH, (CH2)nCOOR, OCONR(CH2)nOR, OCONR(CH2)nNR2, NR(CH2)nNR2, N((CH2)nXR)CO(CH2)nAr, N(R)(CH2)nN(R)COOR, XCOO(CH2)nNR2, OSO2A, OSO2CF3, OSO2-aryl, OCONR2 or OCH2(CH2)nNR2; Q5> = 2- or 3-oxo-piperidino, 3,3,5,5- or 2,2,6,6-tetra-(R)-cyclohe xyl or 3,3,5,5-tetra-(R)-piperidino, all having CH2 in the 4-position replaced by Z, or R1>-substituted 2-oxo-pyrrolidino, cyclopentyl, pyrrolidino (optionally substituted by NR2 or in the 3-position by NA2), R1>-substituted 2-thienyl, 1H-imidazol-1-yl or 1H-1,2,4-tetrazol-1-yl; Q6> = Ar or R1>; Q7> = CO(CH2)nAr; Z = CH2, X, CHCONH2, CH(CH2)n-Q2>, NCO, NCOOR, N(CH2)nOH, CHNH2, C(OH)R, CHNCOR, N(CH2)nCOOR, N(CH2)nCONR2, XCONR(CH2)nNR2, N((CH2)XCOOR)-CO(CH2)nAr, N((CH2)nXR)-Q3>, N((CH2)nNRCOOR)CO(CH2)nAr, N((CH2)nNR2)-Q4>, O(CH2)nNR2, X(CH2)nNR2 or NCO(CH2)nNR2; R6> = Ar (optionally substituted by one or more of Ar (optionally substituted by halo, NO2, CN, A, OR, OCOR, COR, NR2, CF3 , OCF3 or OCH(CF3)2), halo, NO2, CN, OR, A, (CY2)nOR, OCOR, (CY2)n-COOR, (CY2)n-CN, NCOR, COR or (CY2)n-NR2)); R7> = COR, CONR2, COOR, H or A; m = 0-2, and n = 0-7. Independent claims are also included for: (1) the preparation of (I); and (2) mixtures of compounds (I) with each other or with bis-aromatic compounds of formula (V) (specifically pentamidine or its salt) or their analogs or metabolites. Y', Z' = O or N; R9>, R10> = H, OH, halo, 1-10C alkoxy, OCF3, NO2 or NH2; n = 2-6, and R8>, R11> (in m- or p-position) = -C(NH2)=NH, -C(NH2)=NOH, imidazolin-2-yl, 1-methyl-imidazolin-2-yl or tetrazol-5-yl. [Image] - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : Mitotic motor protein inhibitor; Mitotic motor protein regulator; Mitotic motor protein modulator. In a test, 3,4-tetrahydropyrano-fused 6-tert. butyl-2-(3-thienyl)-1,2,3,4-tetrahydroquinoline derivative (Ia) inhibited the cell cycle of HCT cells, typically in presence of 0.4 mu M the cells were in 7% G1, 7% S and 86% G2/M p
US20130123477 Tiacumicin Production Methods, processes and materials for the production and recovery of Tiacumicins produced by culturing a microorganism belonging to the species Dactylosporangium aurantiacum subspecies hamdenensis having the ability to produce and accumulate one or more Tiacumicin in a nutrient medium comprising a carbon source, a nitrogen source, trace elements such as inorganic salts, and an adsorbent, wherein said nitrogen source comprises fish powder, and wherein said Tiacumicin is produced in a yield greater than about 50 mg/L broth.
WO2008040097A1 Furanone compounds and lactam analogues thereof The present invention provides a compound of formula I and a compound of formula II, methods of use and formulations thereof.
US7683078 Neuronal disorders, autoimmune diseases, cancer, cardiovascular diseases; such as 4-Chloro-N-{5-[1-(4-trifluoromethyl-benzyl)-piperidin-3-ylsulfamoyl]-25 thiophen-2-ylmethyl)-benzamide The present invention relates to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Formula (I) IAr1 is a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ar2 a substituted or unsubstituted arylene or heteroarylene group; R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C6-alkyl group.
WO2010109230A1 Novel prodrugs The present invention relates to novel prodrug compounds, or pharmaceutically acceptable salts thereof, which convert in vivo to the active species 4-(1-benzenesulfonyl-6-fluoro-1H-indol-2-yl)-4-hydroxy-cyclohexa-2,5-dienone. The prodrug compounds of the invention have dramatically improved solubility relative to 4-(1-benzenesulfonyl-6-fluoro-1H- indol-2-yl)-4-hydroxy-cyclohexa-2,5-dienone and, accordingly, can be easily formulated for administration to a patient. The prodrugs of the invention are therefore useful for the treatment cellular proliferation disorders, such as cancer.
US7018624 Delivery of poly(ethylene glycol)-modified molecules from degradable hydrogels A degradable PEG hydrogel is described that, upon hydrolysis, releases conjugates of substantially non-peptidic polymers and biologically active molecules. For example, PEG and protein conjugates can be released in vivo from the hydrogels for therapeutic application.
CN102379835A Toilet water with medicinal function The invention relates to toilet water with the medicinal function, which is characterized by being prepared by chilopods, camphor, essence and alcohol in the concentration of 50 percent, and the preparation proportion is as follows: 1-4 chilopods, 1.5-3g of the camphor, 10-20g of the essence, 300-500g of the alcohol and 1-3g of black ants. According to the formula, the chilopods, the camphor and the black ants are placed in the alcohol and the essence for hermetic soaking, the mixture is stored in the shade, and unsealing can be performed after one month for filling. The toilet water has the effects of relieving itching, reliving pain, removing blood stasis, promoting blood circulation and the like and has good efficacy and rapid onset of action for traumatic injuries, dermatalgia, innominate swelling and pain, rheumatic diseases and the like, and the wound surface can restore the smoothness without scarring after using the toilet water. The toilet water is easy in raw material acquisition, low in manufacturing cost, wide in range of applications and convenient to external application and use, and has no side effects.
CN101768132A Biphenyl compound and preparation method and purposes thereof The invention discloses a biphenyl compound with a structural formula as shown below, and a preparation method and purposes thereof. Biological tests have shown that the compound can significantly prohibit the activity of protein tyrosine phosphatase PTP1B. Therefore, the biphenyl compound of the invention can serve as the inhibitor of protein tyrosine phosphatase, and is used to prevent or symptomatically treat diabetes or obesity.
CA2324077C Medicament for preventing and/or treating a mammary carcinoma, containing a steroidal aromatase inhibitor The invention relates to the use of a steroidal aromatase inhibitor for producing a medicament formulated for topical use, for preventing and/or treating a mammary carcinoma. The inventive medicament provides a way of avoiding the side effects associated with systematic use. It is therefore possible to carry out a primary preventative treatment or else a secondary preventative treatment after the appearance of a mammary carcinoma.
CN102977145A Phosphoinositide compounds and their preparation method and use The invention discloses phosphoinositide compounds, a preparation method of the phosphoinositide compounds and a use of the phosphoinositide compounds in preparation of antitumor drugs. Through non-small cell lung cancer cells, a test on a cancer cell growth inhibition activity of the phosphoinositide compounds is carried out and a test result proves that the phosphoinositide compounds have a high cancer cell growth inhibition activity and an inhibition activity of some of the phosphoinositide compounds is comparable to that of cis-platinum and thus the phosphoinositide compounds have good cellular permeability and phosphatidase stability and can be used for exploitation of antitumor drugs.
CN103070875A Composition with anticancer effect The invention provides a composition with an anticancer effect, and the composition mainly comprises the following active components: 2-eeoxy-D-glucose and ursolic acid derivatives. The composition can effectively increase the concentration of active drugs on a tumor site, effectively kill hepatoma carcinoma cells and reduce the toxicity and side effect on normal cells, so that the integral effect for treating the tumor can be improved, and a promising application prospect in treating the solid tumor can be realized.
EP2281554A1 Eye drop composition comprising ketotifen The present invention describes an autoclavable ophthalmic composition comprising ketotifen.
US8182791 Free-flowing fine particle mixtures comprising carrier particles, active drug particles and stabilizer particles, for respiratory system disorders; medical equipment A formulation for an inhaler device comprises carrier particles having a diameter of at least 50 μm and a mass median diameter of at least 175 μm; active particles; and additive material to which is able to promote release of the active particles from the carrier particles on actuation of the inhaler device. The formulation has excellent flowability even at relatively high fine particle contents.
CN101824025A Sulfur-containing diterpene compound, preparation method and medicament combination The invention relates to a sulfur-containing diterpene compound, a preparation method and a medicament combination. The compound has a formula (I), wherein R is hydrogen, and acceptable salt in pharmacy or R is alkyl of C1-C8. The invention also relates to a preparation method of the compound having the formula (I), a medicament combination taking the compound as the active component and the medical purpose in the aspect of anti-inflammation.
CN102846599A External-use composite The invention provides an external-use composite containing at least one compound (a) selected from hydroquinone and derivatives thereof, vitamin, ascorbic acid accounting for 3 to 40 percents of the total weight of the compound, and salts thereof, and crosslinking polyglycerol modified siloxane (b). Although the external-use composite contains the component of (a), the use sense and the stability are good in the meanwhile of inhibiting coloring.
CA2563116A1 Methods for treating or preventing anemia or thrombocytopenia using a triheterocyclic compound The present invention relates to methods useful for treating or preventing anemia or thrombocytopenia, comprising administrating an effective amount of a Triheterocyclic Compound to a subject in need thereof. The present invention also relates to methods useful for preventing anemia or thrombocytopenia in a subject, comprising administrating an effective amount of a Triheterocyclic Compound to the subject, wherein the subject is at heightened risk of developing anemia or thrombocytopenia.
US20130237605 Compositions, methods, and kits for regulating energy metabolism The present invention provides for compositions, methods and kits for regulating energy metabolism. In one aspect, the invention provides for compositions that comprise a combination of (a) branched chain amino acids, such as leucine, and (b) vitamin B6, or any precursors or metabolites of (a) or (b). These combinations may be synergistic and/or effective for reducing weight or adipose volume. In another aspect, the invention provides for methods of regulating energy metabolism by the administration of one or more compositions comprising branched chain amino acids and vitamin B6. The invention also provides for kits comprising compositions of branched chain amino acids and vitamin B6 packaged in an oral dose form with usage instructions.
EP1181283B1 Diaminothiazoles and their use for inhibiting protein kinases Diaminothiazole compounds of formula (I) that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
US20110077252 Pyridyl derivatives, their preparation and use The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1α (HIF-1α) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1α pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-α.
WO2005032556A1 Method for reducing pain The present invention is direct to a method of producing analgesia in a mammalian subject. The method includes administering to the subject an omega conopeptide, preferably ziconotide, in combination with an analgesic selected from the group consisting of morphine, bupivicaine, clonidine, hydromorphone, baclofen, fentanyil, buprenorphine, and sufentanil, or its pharmaceutically acceptable salts thereof, wherein the ω-conopeptide retains its potency and is physically and chemically compatible with the analgesic compound. A preferred route of administration is intrathecal administration, particularly continuous intrathecal infusion. The present invention is also directed to a pharmaceutical formulation comprising an omega conopeptide, preferably ziconotide, in combination with an analgesic selected from the group consisting of morphine, bupivicaine, clonidine, hydromorphone, baclofen, fentanyl, buprenorphine, and sufentanil.
WO2010033978A2 IMIDAZO[1,2-α ]PYRIDINYL BISPHOSPHONATES Novel imidazo[1,2-α]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
US20110112144 Methods of preparing substituted heterocycles The present disclosure relates to methods of preparing substituted thiophenes, which are useful for the treatment and prevention of cancers. Also disclosed are substituted thiophenes made by the methods disclosed herein.
CN102690445A Mycobacterium polysaccharide, its preparation method and application The invention relates to mycobacterium polysaccharide. Its preparation method comprises the following steps of: culturing mycobacterium for 15-25 days, collecting pellicle, successively degreasing, adopting ultrasound-assisted boiling water extraction and centrifuging; extracting residues by the use of dilute base and neutralizing; removing protein from an extract, followed by ethanol precipitation to obtain crude polysaccharide, passing through an ion exchange column, performing dialysis, condensing, and performing freeze drying to obtain mycobacterium polysaccharide. The obtained product is a heteropolysaccharide compound or pure polysaccharide. The weight average molecular weight is 10,000-100,000. Monosaccharide is composed of mannose, glucose, galactose, arabinose and the like. The overall yield can reach 20-30mg/L of a nutrient solution. The purity of the polysaccharide finished product is high. The technology is simple. The quality of the product is stable. The preparation method requires low cost and is easy for industrial production. The mycobacterium polysaccharide has a high antineoplastic activity and can be used to prepare medicines or health products for raising immune functions and resisting tumors.
US20080260829 Bone morphogenic proteins (bmp); cell adhesion modulating agent; peptidomimetics of cyclic peptides comprising classical cadherin cell adhesion recognition (CAR) sequences; modulate cell adhesion and improve drug delivery This invention relates to BMP fusion genes, BMP fusion proteins. The invention further relates to methods for treatment using BMP fusion genes and BMP fusion proteins. Additionally, the invention relates to BMP fusion gene and BMP fusion protein pharmaceutical compositions.
EP1689370B1 METHOD FOR THE PRODUCTION OF A SOLID, ORALLY APPLICABLE PHARMACEUTICAL COMPOSITION COMPRISING 5-Chlor-N ( { (5-2-oxo-3- [4- (3-oxo-4-morpholinyl)-phenyl]-1, 3- oxazolidin-5-yl}-methyl)-2-thiophencarboxamide The invention relates to a method for producing a solid, orally applicable pharmaceutical composition containing 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophen carboxamide in a hydrophilized form, and the use thereof for preventing and/or treating diseases.
CN103040805A Medical application of fargesin The invention relates to the field of medicine, and in particular relates to a medical application of fargesin. The fargesin can be used for preventing and treating enteritis.
CN101671385A Triterpene glycosides antifungal compounds of sea cucumber HolotoxinD-I and preparation method thereof The invention relates to the technical field of medicines, particularly to six triterpene glycosides antifungal compounds HolotoxinD-I separated from a sea cucumber. The chemical structural formula isas follows on the right. An in vitro anifungal experiment shows that the compounds have obvious inhibitory effect on Candida ablbicans SC5314, Cryptococcus neoformans BLS108, Candida tropicalis, Trichophyton rubrum, Mircrosporum gypeseum and fuming Aspergillus. The invention can provide leading compounds for developing novel antifungal drug, and has a significant value on exploiting and using marine medical resources in China.
WO2014023027A1 Erlotinib hydrochloride polymorph and preparation method therefor Disclosed in the present invention are an Erlotinib hydrochloride polymorph and the preparation method therefor. In particular, disclosed in the present invention are an Erlotinib hydrochloride semihydrate polymorph with a purity ≥95% and the preparation method therefor. The preparation method of the present invention is simple to operate and suitable for industrial production. The polymorph prepared by the preparation method of the invention has the advantages of good stability and high water solubility.
CN102631350A Compound preparation of quetiapine fumarate and lurasidone The invention discloses a compound preparation of quetiapine fumarate and lurasidone, which is used for treating schizophrenia. Each preparation unit contains the quetiapine fumarate with the effective dosage of 25-300mg and the lurasidone with the effective dosage of 20-100mg. The dosage of the compound preparation is obviously lower than those of other medicines which are singly used, and the compound preparation has the function of synergy, so that the compound preparation is suitable for severe schizophrenia patients.
US20090274737 Implant comprising a surface of reduced thrombogenicity An implant for a human or animal body, comprising a surface having reduced thrombogenic properties, whose surface has a wetting angle of Θ, where Θ≦80°. Also disclosed is a method for producing an implant and the use an implant to reduce the dose or concentration in administration of a concomitant systemic medication with one or more anticoagulant active ingredients before, during or after implantation of the implant in a human or animal body.
WO2014029327A1 Prodrug of green tea epigallocatechin-3-gallate (pro-egcg) for use in the treatment of endometriosis Method of treating endometriosis and related indications, comprising the administration of Pro-EGCG, a synthetic and derivative product of epigallocatechin-3-gallate [(-)-EGCG]. Use of Pro-EGCG in the manufacture of a medicament for treating endometriosis and related indications. Pro-EGCG for use in the treatment of endometriosis and related indications.
CN1660056A Oral disintegration tablet of tramadol hydrochloride and preparation method An orally disintegrating tablet of tramadol hydrochloride is prepared through preparing the dispersed solid from tramadol hydrochloride and dispersing solid carrier, mixing it with filler, disintegrant, flavouring and lubricant, stirring and tabletting.
US20100192945 Inhalation devices and related methods for administration of sedative hypnotic compounds An inhalation device for administering one or more sedatives via pulmonary delivery for treating a sleep disturbance.
WO2012087782A1 Pyrazolopiperidine compounds as ccr1 receptor antagonists Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
CN101574356A Tenofovir disoproxil pharmaceutical salt and preparations thereof The invention relates to an adenine (tenofovir disoproxil) salt containing 9-[(R)-2-[[double[[(isopropoxy carbonyl) oxyl] methoxy] phosphinyl] methoxy] propyl] or medicaments of pharmacological activated derivatives thereof. The invention provides a tenofovir disoproxil pharmaceutical salt and a synthesis technology of the pharmacological activated derivatives of the tenofovir disoproxil pharmaceutical salt and also relates to a preparation technology of the pharmaceutical preparations containing the tenofovir disoproxil pharmaceutical salt and the rmacological activated derivatives thereof. The preparations can be used for administration on patients for curing or preventing Type B viral hepatitis or human immunodeficiency virus (HIV/AIDS) infection and HBV or HIV mutant infection with drug tolerance to nucleoside inhibitors and non-nucleoside inhibitors.
WO2009031919A1 Alcoholism recurrence preventing agent and method for the use thereof The invention relates to medicine, in particular to alcoholism recurrence preventing agents and to methods for the use thereof. The inventive alcoholism recurrence preventing agent contains a cyanamide and polylactide mixture with a component ratio (mass) ranging from 10:90 to 40:60. The inventive method for preventing alcoholism recurrences consists in intramuscularly injecting to a patient, in general once per month, a solution containing the cyanamide and polylactide mixture in a single dose of 0.5-1.5 g. The agent produces a substantial retardation effect and a low effective agent release.
CN101959523A Antimicrobial agent for gram-positive bacteria Disclosed is a novel antimicrobial agent for Gram-positive bacteria extending beyond the mechanism of bacterial drug resistance. The antimicrobial agent contains, as active ingredients, particles which adhere to a Gram-positive bacterial cell wall and do not adhere to a mammalian cell membrane, have a particle diameter of 5 [mu]m or less, and practically do not contain an antimicrobially active component against Gram-positive bacteria. According to the antimicrobial agent of the invention, antimicrobial effect also on Gram-positive bacteria showing multidrug resistance typified by MRSA and VRE can be achieved. Further, the emergence of new multidrug resistant bacteria which becomes a major problem in the use of an antibiotic can be avoided.
WO2011134191A1 Compound pharmaceutical formulation A compound pharmaceutical formulation is disclosed by the present invention, characterized in that it contains levoamlodipine or pharmaceutically acceptable salts thereof, and pravastatin. The compound pharmaceutical formulation of levoamlodipine and pravastatin in the present invention has hypotensive effect and lipid-reducing effect as well. The combination of the two components can exert a synergistic effect, and control both the blood pressure and blood fat in patient effectively.
US20080032985 4-Substituted Quinoline Derivatives, Method and Intermediates for Their Preparation and Pharmaceutical Compositions Containing Them The present invention relates to 4-substituted quinoline derivatives of general formula I: which are active as antimicrobials. The invention also relates to the method and intermediates for their preparation and the pharmaceutical compositions containing them.
EP1501799A1 Compounds useful in preparing camptothecin derivatives Novel compounds are provided having formula (I) and salts thereof, where R1 is hydrogen, an alkyl, aralkyl, hydroxymethyl, carboxymethyl, acyloxymethyl or trialkylsilyl group, or a group -CH2NR3R4 where N is a linking nitrogen atom and where (a) R3 and R4 are independently selected from hydrogen and alkyl, alkenyl, hydroxyalkyl and alkoxyalkyl groups; (b) R3 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group, and R4 is -COR5 where R5 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group; or (c) R3 and R4 taken together with the linking nitrogen atom form a saturated 3- to 7-member heterocyclic group. These compounds are useful intermediates in a process to prepare camptothecin derivatives including the anti-cancer drug irinotecan.
CN1865260A Long chain arylpiperazine modified duloxetine analog compound and preparation and uses The invention discloses a long chain aromatic piperazidine decorative duluoxidin similar compound and making method and appliance, which is characterized by the following: the compound feature is in the structural formula (1); the making method of structural formula (2) comprises the following steps: reacting duluoxidin or N-R1 replacement duluoxidin and chlorohydrocarbon chloral to produce amide in the chloroform at room temperature under the action of acid-attaching agent; reacting the produce and aromatic piperazidine to produce long chain aromatic piperazidine amide; deacidizing the long chain aromatic piperazidine amide to produce long chain aromatic piperazidine duluoxidin similar compound through lithium aluminum hydride in the tetrahydrofuran. The invention can produce antidepressant drug, which is simple to manufacture and operate.
WO2012021455A1 Cyclic boronic acid ester derivatives and therapeutic uses thereof Disclosed herein are antimicrobial compound compositions, pharmaceutical compositions, the use and preparation thereof. The invention relates to cyclic boronic acid ester derivatives of formula I and their use as therapeutic agents particularly in the treatment of bacterial infections.
WO2012037484A1 Ester pro-drugs of [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol for treating skin diseases and conditions The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl] methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.
WO2007128752A1 Pyridyl compounds Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
CN103040853A Application of gardenia sesou as vision care drug ingredient The invention provides an application of a new ingredient-gardenia sesou as a vision care drug ingredient. The drug can improve the blood circulation of eyes, protect the retina against the harm of ultraviolet visible light, effectively protect the eyes, and prevent and reduce the possibility of myopia, hyperopia and amblyopia, and the preparation is simple. The gardenia sesou is a new-structural compound which is extracted and separated from gardenia, and the molecular formula of the gardenia sesou is C42H60O14. The gardenia sesou can be applied to the field of vision care.
CN101991605A Medicament for bactriostasis, protection and cleaning of vagina of human body and preparation method thereof The invention relates to a medicament for bactriostasis, protection and cleaning of the vagina of a human body and a preparation method thereof. The medicament is mainly prepared from water soluble pearl powder, matrine, chlorhexidine acetate, borneol and an auxiliary material according to weight proportion. Compared with the prior art, the invention has the advantages that the medicament has obvious and strong effect of inhibiting staphylococcus aureus and Candida albicans, takes effects rapidly and inhibits the staphylococcus aureus and the Candida albicans by over 90 percent after taking effect for 2 min; the product contains the water soluble pearl powder and has the effects of clearing heat, detoxicating, sterilizing, disinfecting, stopping bleeding and strengthening muscle; the pH value of the product is consistent with the pH value of the vagina of the human body, and the balance of a bacterium group in the vagina can be improved and maintained; and when in use, the product is arranged in the position at a distance of 7-8cm from the vagina, is convenient for use and is used by one pill once every three days.
WO2009058944A3 Nonsteroidal compounds useful as modulators of glucocorticoid receptor ap-1 and /or nf- kappa b activity and use thereof Disclosed are compounds of Formula (I) wherein: one of A and D is -N- and the other of A and D is -C-; or enantiomers, diastereomers, or pharmaceutically-acceptable salts thereof. Also disclosed are methods of using such compounds to modulate the function of glucocorticoid receptor activity and pharmaceutical compositions comprising such compounds.
US20080119513 To treat osteoarthritis; matrix metalloproteinases-13 inhibitors It is considered that MMP-13 inhibitors contribute to the treatment or prevention against the diseases caused by or related to activity of MMP-13, especially osteoarthritis (OA). Therefore, the development of MMP-13 inhibitors has been desired. A compound represented by the general formula (I): wherein Z is 1,4-phenylene and the like; R1 is hydroxy and the like; R2 is hydrogen atom, optionally substituted lower alkyl, and the like; R12 is hydrogen atom; or R2 and R12 taken together with the adjacent carbon atom may form a ring; R3 is hydrogen atom, optionally substituted lower alkyl, and the like; R4 is halogen, lower alkyl, and the like; m is 0, 1, or 2; X is a bond, —C≡C—, and the like; Y is optionally substituted phenyl, optionally substituted naphthyl, and the like, its optically active substance, their pharmaceutically acceptable salt, or a solvate thereof.
CN1809531B Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators The present invention provides compounds of formula (I), wherein X, a, b, R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
WO2013115740A1 Synergisctic combination comprising a meglitinide derivative and lipoic acid The present invention relates to pharmaceutical compositions comprising a meglitinide derivative agent and alpha-lipoic acid that shall be used in the treatment of type 2 diabetes.
WO2014045162A1 ALKYL-SUBSTITUTED HEXAHYDROPYRANO[3,4-d] [1,3]THIAZIN-2-ANIME COMPOUNDS Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
CN102531946A 3-methoxybenzamide (MBA) derivant as well as preparation method and application thereof The invention discloses a 3-methoxybenzamide (MBA) derivant, which is disclosed in the following structural formula (1), wherein R1 is chlorine or bromine, R2 and R3 are independently fluorine or hydrogen, and n is an integer of 1-5. According to the 3-MBA derivant, a hydrophobic halogenated hydrocarbon side chain of which the length is 3-7 atoms is introduced on the C-3 site of 3-MBA to discover the optimal length of the hydrocarbon side chain introduced on C-3 of the 3-MBA. Meanwhile, a chlorine atom and a bromine atom with better lipid solubility are introduced into the tail end of the side chain so as to enhance the antibacterial activity of the derivant. In order to improve the target and the antibacterial activity of a compound, fluorine atoms are introduced onto the C-2 site and the C-6 site of the 3-MBA. The experiment proves that the compound disclosed by the invention can be used for specifically inhibiting the activity of various pathogenic bacteria even drug resistant bacteria, such as staphylococcus aureus, staphylococcus epidermidis, staphylococcus haemolyticus, staphylococcus saprophyticus, bacillus subtilis, bacillus anthracis and the like.
WO2014151386A1 Salts and solid forms of isoquinolinones and composition comprising and methods of using the same Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, solid forms thereof, and pharmaceutical compositions thereof.
EP2066355A2 Combination comprising a peroxisome proliferator activated receptor agent and a second neurogenic agent for treating a nervous system disorder, increasing neurodifferentiation and increasing neurogenesis The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system including by stimulating or increasing neurogenesis, neuroproliferation, and/or neurodifferentiation. The disclosure includes compositions and methods based on use of a peroxisome proliferator-activated receptor (PPAR) agent, optionally in combination with one or more other neurogenic agents, to stimulate or increase a neurogenic response and/or to treat a disease.
CN103479594A Imidafenacin film-coated tablet and preparation method thereof The invention provides an imidafenacin film-coated tablet. The imidafenacin film-coated tablet comprises raw and auxiliary materials in parts by weight as follows: 1-5 parts of imidafenacin, 700-850 parts of pregelatinized starch, 600-700 parts of microcrystalline cellulose, 3-6 parts of lubricants and appropriate coating agents. The invention further provides a preparation method of the film-coated tablet. According to research findings, the imidafenacin can dissolve completely even in 5min in a specific prescription ratio of the tablet; meanwhile, a specific fluidized bed granulation process is adopted, so that the uniformity of the content of the imidafenacin in the preparation can be remarkably improved; and the content of main drugs in the imidafenacin tablet is quite low, so that the quality uniformity of drugs is well guaranteed with the preparation method.
US20060094660 Inhibitor of the shh signalling patway and a testosterone supressing agent for the treatment of cancer A method of protecting a patient from possible adverse effects of a treatment involving inhibition of the SHH-signalling pathway in the patient, the method comprising suppressing testosterone or its effect in the patient. A method of treating a proliferative disease such as cancer in a patient the method comprising inhibiting the SHH-signalling pathway and suppressing testosterone or its effect in the patient. Typically, the SHH-signalling pathway is inhibited using cyclopamine or a derivative thereof, and testosterone is suppressed using any one or more of a GnRH antagonist, a GnRH agonist, an androgen antagonist or a Sa-reductase inhibitor.
CN103127091A Application of Aphanamixoid A in medicines curing colorectal cancer The invention discloses application of Aphanamixoid A in medicines curing colorectal cancer and belongs to the medicines new use technical field. An in vitro MTT antineoplastic activity evaluation shows that the Aphanamixoid A has evident inhibiting effect on growth of human colorectal cancer cell strain LOVE1, LoVo, SW620 and SW480. Therefore, the Aphanamixoid A can be used for preparing colorectal cancer resisting medicines, and has good development and application prospect. Due to the fact that use of the Aphanamixoid A in preparation of the medicines curing the colorectal cancer is made public for the first time, and the skeleton type is completely novel, the Aphanamixoid A has an unexpectedly high colorectal cancer cell inhibitory activity.
US20100093699 Compounds and uses thereof - 177 This invention relates to novel compounds having the structural Formula (I) below: and their pharmaceutically acceptable salts, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence, and neurodegenerative disorders.
WO2012092484A2 Substituted purine nucleosides, phosphoroamidate and phosphorodiamidate derivatives for treatment of viral infections This invention is directed to novel compounds of formula (I) having the structure (I) wherein U, V, W, Z, R 1, X1, X2, and Y are defined herein. The compounds of formula (I) and pharmaceutical compositions containing these compounds are useful in the treatment of viral infections in mammals mediated, at least in part, by a virus in the Flaviviridae family of viruses, in particular hepatitis C virus (HCV).
EP1450785B1 Method of treating dermatoses using avermectin compound A method for treating dermatoses including transient acantholytic dermatitis, acne miliaris necrotica, acne varioliformis, perioral dermatitis, and acneiform eruptions is disclosed. The method includes topical application of a dermatological composition containing an avermectin compound to the affected areas of a patient.
CN101579347A Breast perfusion preparation for treating mammitis of milk cow in lactation period and preparation method thereof The invention provides a breast perfusion preparation for treating mammitis of milk cow in lactation period, which belongs to the field of medical preparation for veterinary use; every 3g of the perfusion preparation contains 150-250 mg of amoxicillin, 50-125 mg of sulbactam, 5-15 mg of prednisolone and the rest of substrate; the substrate contains 0.1-12% of suspending aid, 0.1-2% of wetting agent, 0.01-1% of antioxidant, 0.05-1% of preservative and the rest of dispersion medium; the invention can be obtained via the following steps: firstly, dissolving or dispersing suspending aid, antioxidant, wetting agent and preservative into proper amount of dispersion medium, then slowly adding the rest of the dispersion medium into a colloid mill to obtain the substrate, adding medicine into the substrate, grinding via the alternating method of circularly grinding and non-circularly grinding. The preparation of the invention is simple in preparation technique, easy to realize industrialization, low in production cost, low in expenditure for treatment, low in toxicity, wide to use and high in efficiency; the invention can be clinically used for treating mammitis in lactation period caused by Gram positive bacterium and Gram negative bacterium.
EP2497473A1 Therapeutically effective amounts of R(+) and S(-) pramipexole for use in the treatment of Parkinson's disease and pharmaceutical compositions thereof There is provided a pharmaceutical composition comprising a therapeutically effective amount of R(+) pramipexole and a therapeutically effective amount of S(-) pramipexole, wherein said therapeutically effective amount of R(+) pramipexole is 50 milligrams plus or minus 10% to 5,000 milligrams plus or minus 10% and wherein said therapeutically effective amount of S(-) pramipexole is 0.125 milligrams plus or minus 10% to 4.5 milligrams plus or minus 10%, and therapeutically effective amounts of R (+) and S(-) pramipexole for use in the treatment or prevention of Parkinson's disease or the symptoms thereof.
US20050176828 Polyamine acylated with a hydrophobic acyl group, where acylation is by formation of either an amide or a sulfonamide linkage; antiproliferative agents; inhibition of cellular polyamine synthesis, even in the presence of exogenously supplied spermidine to inhibit cell growth and proliferation The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.
US7410995 N-linked sulfonamide of heterocyclic thioesters for vision and memory disorders This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using N-linked sulfonamides of heterocyclic thioesters.
WO2006114702A2 Pharmaceutical compositions and methods comprising a combination of a selective estrogen receptor modulator and an aromatase inhibitor The present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof a combination of a 2-(-)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol or a pharmaceutically acceptable salt or prodrug thereof and an aromatase inhibitor. Particularly, the present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof (-)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8- tetrahydronaphthalene-2-ol or a pharmaceutically acceptable salt or prodrug and an aromatase inhibitor selected from aminoglutethimide; formestane; atamestane; anastrazole; fadrozole; finrozole; letrozole; vorozole; 4-[N-(4-bromobenzyl)-N-(4-cyanophenyl)amino]-4H-1,2,4-triazole or exemestane, or a pharmaceutically acceptable salt thereof.
CN103052636A D2 antagonists, methods of synthesis and methods of use Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.
US8372449 Method for enhancing the DNA repair process, treating disorders associated with the DNA repair process, enhancing antitumor response and treating disorders associated with anti-tumor response in mammals by administering pruified quinic acid and/or carboxy alkyl ester The disclosure provides a method for isolating the bioactive component of the water-soluble extract of Uncaria tomentosa known as C-MED-100®, comprising (i) precipitating the spray drying carrier from C-MED-100®; (ii) using the resulting C-MED-100® to obtain a spotting mixture for thin layer chromatography (TLC); (iii) spotting the C-MED-100® spotting mixture on pre-run TLC plates and eluting the plates to obtain the fluorescing band with Rf=0.2-0.3; (iv) scraping off the Rf=0.2-0.3 band, eluting it in ammonia and freeze drying the eluted band to form a powder; and (v) extracting the powder with methanol to remove solubilized silica gel, concentrating the methanol solution and crystalizing the concentrated solution to obtain the bioactive component. The isolated bioactive component in vitro is a quinic acid analog, preferably quinic acid lactone. By contrast, the disclosure further shows the isolated bioactive component in vivo is quinic acid, whether as free acid or as a quinic acid salt, including quinic acid ammonium salt. The disclosure then provides for a pharmaceutical composition comprising a pharmaceutically effective amount of the bioactive component and a nontoxic inert carrier or diluent. The pharmaceutical composition and bioactive component may be used to enhance immune competency, treat disorders associated with the immune system, inhibit the inflammatory response, treat disorders associated with the inflammatory response, enhance the anti-tumor response, and treat disorders associated with the response to tumor formation and growth, all in mammals.
WO2007098252A3 Methods and compositions for treating hyperalgesia This invention provides compounds which specifically inhibit TRPA1 but not other members of the thermoTRP ion channel family. Also provided in the invention are methods of using TRPA1-specific inhibitors to treat or alleviate pains mediated by noxious mechanosensation.
WO2009004650A1 Novel substituted piperidones as hsp inducers The present invention relates to novel compounds of formula (I) or (II), their pharmaceutically acceptable salts and their hydrates, solvates, stereoisomers, conformers, tautomers, polymorphs and prodrugs and also pharmaceutically acceptable compositions containing them Wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification. The compounds of the present invention are HSP inducers and by virtue of this effect, useful for the treatment of various diseases accompanying pathological stress. The present invention also relates to a process for the preparation of the said novel compounds. The invention also relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.
WO2013017600A1 Substituted 3-(biphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-one The invention concerns substituted 3-(biphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-one, more particularly for therapeutic purposes, pharmaceutical means and the use thereof in treatment, in particular for prophylaxis and for the treatment of tumorous diseases.
CN101417152A Local vascular delivery of mtor inhibitors in combination with peroxisome proliferators-activated receptor stimulators Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the prevention of thrombosis. The drugs, agents, and/or compounds may also be utilized to treat specific disorders, including vulnerable plaque, and athereosclerosis in type 2 diabetic patients. Therapeutic agents may also be delivered to the region of a disease site. In regional delivery, liquid formulations may be desirable to increase the efficacy and deliverability of the particular drug. Also, the devices may be modified to promote endothelialization. Various materials and coating methodologies may be utilized to maintain the agents or compounds on the medical device until delivered and positioned. In addition, the devices utilized to deliver the implantable medical devices may be modified to reduce the potential for damaging the implantable medical device during deployment. In addition, various polymer combinations may be utilized to control the elution rates of the therapeutic drugs, agents and/or compounds from the implantable medical devices.
EP2413940A1 Compositions comprising 2, 4, 6-triamino-1, 3, 5-triazine derivatives for treatment of schizophrenia The present invention is useful for providing an excellent pharmaceutical composition for prevention and/or treatment of schizophrenia, containing a BEC1 potassium channel inhibitor or a pharmaceutically acceptable salt thereof as an active ingredient, and is particularly useful for providing a pharmaceutical composition for prevention and/or treatment of the positive symptoms, negative symptoms, cognitive impairments and the like of schizophrenia.
US20120077842 Quinoline derivative-containing pharmaceutical composition A pharmaceutical composition comprising a compound represented by the formula (I) or pharmaceutically acceptable salt thereof or solvate thereof; and a basic substance is excellent in dissolution, is stable even after a long term storage, and is useful as a preventive or therapeutic agent against a tumor: wherein, R1 is a hydrogen atom, a C1-6 alkyl group or a C3-8 cycloalkyl group; and R2 is a hydrogen atom or a methoxy group.
US7101886 such as N-{2-[2-(4-1,2-Benzisothiazol-3-yl-piperazin-1-yl)-ethyl]-phenyl}-2-(2,5-dimethoxy-phenyl)-acetamide; antagonists of dopamine D2 receptors and of serotonin 2A (5HT2a) receptors; for treatment of depression and dementia/schizophrenia This invention relates to compounds of the formula 1 wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.
CN101919841A Application of eudesmane-type sesquiterpenoids The invention relates to application of eudesmane-type sesquiterpenoids. The sesquiterpenoids are Encelin, and have chemical name of (3aR, 4aR, 8aS, 9aR)-8a-methyl-3,5-dimethylidene-4,4a,9,9a-tetrahydro-3aH-benzo [f] [l] benzofuran-2,6-dione, and molecular formula of C15H16O3. The invention is characterized in that the sesquiterpenoids are applied to medicines for treating leukemia. The eudesmane-type sesquiterpenoids Encelin respectively have remarkable proliferation inhibitory action on the cells of acute and chronic myeloid leukemia and lymphocytic leukemia.
CN103720651A In-situ gel injection containing florfenicol/hydrogenated castor oil The invention relates to an in-situ gel injection containing florfenicol/hydrogenated castor oil drug-carrying granules, which is prepared by the following steps: preparing florfenicol and hydrogenated castor oil into drug-carrying granules, and suspending the drug-carrying granules in an 18-22% poloxamer 407 water solution. The injection has the advantages of simple preparation technique, uniform drug release, favorable biocompatibility, no irreversible injury on tissues in the injection site, and degradable and removable slow-release carrier.
US20060165791 Oral dosage form prepared by forming granules comprising oxycodone hydrochloride, alkyl cellulose and polymethacrylate, and drying said granules; improving efficiency and quality of pain management A method for substantially reducing the range in daily dosages required to control pain in approximately. 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady state conditions. Another embodiment is directed to a method for substantially reducing the range in daily dosages required to control pain in substantially all patients by administering an oral solid controlled release dosage formulation comprising up to about 160 mg of oxycodone or a salt thereof, such that a mean maximum plasma concentration of oxycodone up to about 2.40 ng/ml from a mean of up to about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration up to about 120 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady-state conditions are achieved. Controlled release oxycodone formulations for achieving the above are also disclosed.
CN101199520A Beta-Lacetam anti-biotic compound dose for animal containing benemid The invention relates to a Beta-lactam antibiotic compound preparation for animals, which contains probenecid. Calculated by weight percentage, the preparation is composed of 1 to 20 percent of probenecid , 5 to 20 percent of Beta-lactam antibiotic, 5 to 40 percent of cosolvent, and acceptable vector in pharmacy which is added until the preparation is 100 percent. The preparation can be orally administrated , and can be dissolved in water to be drunk by livestock and fowl. The invention has a broad antifungal spectrum, shows a strong antibacterial activity, is convenient to be used clinically, has good safety, and is applicable to treating light to moderate infection. The used practice shows that the preparation can reduce the dosage of the Beta-lactam antibiotic in clinical practice, can reduce the occurrence possibilities of drug resistance, and can also save the treatment cost with good using effect.
EP2243772A1 Novel P2X7R antagonists and their use The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.
WO2011006653A1 An agent for restoring lost memory on the basis of n,n'-substituted 3,7-diazabicyclo[3.3.1] nonanes The present invention discloses an agent for restoring lost memory or for preventing memory loss or for treating a memory disorder or a learning disorder which comprises an N, N'- substituted 3, 7-diazabicyclo [3.3.1] nonane having the general Formula (1) :
CN101744833A Medicinal composition for treating bacterial vaginitis The invention relates to a medicinal composition for treating bacterial vaginitis, which comprises main medicaments, substrates, a bioadhesive material, a release rate regulator and other additives. The medicinal composition for treating bacterial vaginitis has specific biological adhesion, keeps longer time, reduces leakage of the medicaments, prolongs the contact time of the medicaments and the vagina mucosa, and guarantees the curative effect. The composition has specific vagina slow release performance, and can continuously release the medicaments for 2 to 7 days. Compared with the common preparation, the medicinal composition prolongs the releasing time of the medicaments, can reduce the administration times, and is convenient for the patient to take. As simultaneously the medicinal composition has the characteristics of biological adhesion and slowly-released long effect, the medicinal composition has no requirement for the administration time, and the administration can be carried out at any time.
US20110144155 8-hydroxyquinoline derivatives for the treatment of hematological malignancies The application relates to compositions and methods for treating hematological malignancies and proliferative diseases, disorders and conditions involving increased D-cyclin expression. In particular, the application relates to compositions and methods for treating the hematological malignancies acute myeloid leukemia (AML), lymphoma and multiple myeloma (MM) using 5-nitrogen substituted hydroxy quinolones as well as 7-bromo-5-chloro substituted hydroxy quinolones and 5-chloro substituted hydroxy quinolones.
CN101406460B Euthyrox tablet The invention belongs to the technical field of pharmaceutical preparation, and in particular relates to a levothyroxine sodium tablet. The levothyroxine sodium tablet is characterized in that the tablet comprises the following components in weight portion: 0.05 portion of levothyroxine sodium, 15 to 25 portions of calcium hydrogen phosphate, 18 to 25 portions of microcrystalline cellulose, 4 to 8 portions of dextrin, 0.5 to 4 portions of sodium starch glycollate, and 0.5 to 1 portion of partial glyceride. The compound can obviously improve the stability and dissolution of the preparation, and can benefit the clinical application of the preparation.
EP2621498A2 Combination treatment for dermatological conditions The invention relates to a method of treating dermatological conditions or symptoms associated therewith in a patient in need thereof by topically administering an effective amount of a combination of brimonidine or a pharmaceutically acceptable salt thereof and oxymetazoline or a pharmaceutically acceptable salt thereof to the affected area of skin on the patient. The invention further relates to topical compositions including the combination of compounds and a pharmaceutically acceptable carrier.
CN101129358A Moguisteine sustained-release tablet and method of preparing the same The invention provides a process for preparing moguistein sustained-release matrix tablets, wherein the formula comprises (g/g) moguistein 20-60%, matrix material 10-70%, thinning agent 0-50%, right amount of binding agent and lubricating agent. The preparing process comprises the steps of mixing raw materials with auxiliary materials, then tabletting the powders, or making particles, then mixing with lubricant and tabletting.
CN1586464A Compound ambroxol dripping pill The present invention discloses one kind of orally taken dripping pill preparation with compound medicine components of ambroxol hydrochloride and clenbuterol hydrochloride as active components. The medicine is used in relieving cough, eliminating phlegm and relieving asthma, and has high bioavailability, fast medicine release, fast acting and convenient carrying about. The compound ambroxol dripping pill is prepared with ambroxol hydrochloride and clenbuterol hydrochloride as active components and through mixing with non-ionic surfactant as matrix.
CN103566098A External specific detumescence ointment formula for orthopedics The invention provides an external specific detumescence ointment formula for orthopedics. The external specific detumescence ointment formula for orthopedics is composed of the following two parts: 1) anti-inflammatory analgesic ointment composed of 330 g of radix angelicae pubescentis, 40 g of radix aconite, 165 g of raw arisaema, 60 g of radix dipsaci, 15 g of Chinese honey locust, 2500 g of mirabilite, 29 kg of maltose, 26 kg of talc powder, 7 kg of sodium benzoate and 4 kg of glycerol; and 2) detumescence powder composed of 30 g of lotus leaf, 30 g of radix aconiti kusnezoffii, 30 g of raw pinellia, 15 g of licorice, angelica, 30 g of radix angelicae, 30 g of raw rhubarb, 60 g of radix trichosanthis, 24 g of pericarpium citri reticulatae and 60 g of phellodendri. The external specific detumescence ointment formula for orthopedics provided by the invention is suitable for acute pain and has the functions of activating blood circulation and eliminating swelling, cooling blood and relieving pain, dredging collaterals and setting bone, and when being used for treating acute pain, the external specific detumescence ointment formula for orthopedics can not only accelerate the bone setting time, but also can relieve pin and eliminate swelling.
EP2787001A1 (E)-3-Aryl-3-oxoprop-1-enyl-2-phosphonic acid and its derivatives, methods for their preparation and their use The present invention is (E)-3-aryl-3-oxoprop-1-enyl-2-phosphonic acid and its derivatives in the form of esters or salts, process for their preparation and use as compounds having ability to interact with nucleic acids, including DNA intercalating properties and antitumor activity.
EP1870105A1 Use of fucans in the treatment of psoriasis Compositions, methods and the like comprising fucans such as fucoidan to treat arthritis.
CN101372475B Aromatic heterocyclic substituted acardite derivative and use thereof The invention discloses a compound of general formula (1) or (2) or salt which can be accepted by the compound on pharmacy; wherein, R1 is nitrogen heterocyclic ring except for pyridine; R2 is H, halogen, C1-5 alkyl, C1-5 alkoxy or C1-5 haloalkyl; R3 is H, halogen, C1-5 alkyl, or C1-5 alkoxy. The compound and the salt which can be accepted by the compound on pharmacy can be applied for preparing the medicine for treating tumor or leukemia.
US8088605 Exopolysaccharides delivery system for active molecules The present invention relates to a delivery system for delivery of an active molecule to a patient, the delivery system comprising a population of exopolysaccharide micelles, each micelle defining a core for containing the active molecule.
EP1176959B1 Novel prolines as antimicrobial agents Transfer ribonucleic acid (tRNA) synthetase inhibitors, salts, and pharmaceutically acceptable compositions thereof of general formula (I), wherein Ar is aryl and heteroaryl; L is -C(O)N(Q)CH2-, or -CR?10R11OCR12R13¿-; Q is hydrido, -(CH¿2?)mCO2H and -(CH2)mCO2CH3, m is 1, 2, 3, and 4; R1, R?2, R9, R10, R11, R12 and R13¿ are hydrido or lower alkyl; wherein Het is a heterocyclic moiety, the inhibitors are suitable for use as antimicrobial agents.
US7858312 Method of treating bladder and lower urinary tract syndromes The present invention relates to bladder and lower urinary tract syndromes, particularly, irrative symptoms, and to a method of treating same using α1d-adrenergic receptor (α1dAR) antagonists. The invention further relates to a method of screening compounds for their ability to serve as α1dAR selective antagonists.
WO2007125542A3 A process for preparation of adapalene The present invention discloses a process for preparation of highly pure Adapalene, chemically designated as 6-[3-(l-adamantyl)-4-methoxy phenyl]-2-naphthoic acid (I) comprising: a) reacting 1-adamantanol with 4-bromophenol (II) in presence of sulphonic acid with or without the use of organic solvent to give 2-(l-adamantyl)-4- bromophenol (III); b) alkylating compound of formula(III) with dimethylsulphate in presence of base in organic solvent to obtain 2-(l-adamantyl)-4-bromoanisole (IV); c) C-C coupling the compound of formula (IV) with methyl-6-bromo-2- naphthoate using magnesium, purified zinc chloride and NiCl2-DPPE in THF at a temperature of 40-60°C tO obtain methyl ester of 6-[3-(l- adamantyl)-4-methoxy phenyl] -2-naphthoic acid (V); d) purifying crude methyl ester of 6-[3-(l-adamantyl)-4-methoxy phenyl]-2- naphthoic acid (V) using a mixture of organic solvent to obtain pure compound (V); e) hydrolyzing the compound (V) with a solution of alkali in organic solvent to obtain metal salt of 6-[3-(l-adamantyl)-4-methoxy phenyl] -2-naphthoic acid (VI); f) acidifying metal salt of adapalene (VI) using organic or inorganic acid to obtain crude adapalene (I) and g) recrystallizing the crude adapalene (I) using a mixture of organic solvents to obtain pure adapalene (I).
WO2009124950A3 4-methyl-4,5-dihydro-1h-pyrazole-3-carboxamide useful as a cannabinoid cb1 neutral antagonist The present invention relates to 4-methyl-4, 5-dihydro-1H- pyrazole-3-carboxamide, and pharmaceutically acceptable salts and solvates thereof. It further concerns pharmaceutical compositions comprising this compound as active ingredient as well as processes and intermediates for preparing this compound and compositions. The referred compound is a cannabinoid CB1 neutral antagonist useful in the prophylaxis and treatment of food intake disorders.
CN102178672A Medicinal composition for treating esophageal cancer or nasopharyngeal darcinoma, and application, kit and packaging piece The invention relates to a medicinal composition for treating esophageal cancer or nasopharyngeal darcinoma, and application, a kit and a packaging piece. The medicinal composition, the kit and the packaging piece comprise Lobaplatin with treatment effective dose and Docetaxel with treatment effective dose which serve as a combined preparation to be used simultaneously, separately and sequentially. The medicinal composition, the kit and the packaging piece can achieve excellent curative effect and have small toxic or side effect when used for treating esophageal cancer or nasopharyngeal darcinoma.
WO2008008821A3 Use of trifluoromethyl substituted benzamides in the treatment of neurological disorders The invention relates to methods of using the compounds of the invention, including trifluoromethyl substituted benzamide compounds and salts thereof, as well as pharmaceutical compositions comprising the same, in the treatment of Eph receptor-related (e.g., neurological) injuries and disorders. The invention also relates to modulating the activity of an Eph receptor in a cell, stimulating neural regeneration, and reversing neuronal degeneration, by administering a compound of the invention to a cell or subject in an effective amount.
US7834005 anticancer, antiviral, antibiotic use; new derivatives of anthramycin class of antitumor antibiotics Disclosed are compounds of Formula I wherein X, Y, R1-R7, T1, T2, Z, and p are as described herein; a pharmaceutical composition comprising a compound of Formula I and a carrier; a method of inhibiting growth of a cell, which method comprises administering in an amount effective to inhibit growth a compound of Formula I; a method of treating cancer in a mammal, which method comprises administering in an amount effective to treat cancer a compound of Formula I; a method of treating a viral, parasitic, or bacterial infection of a cell, which method comprises administering in an amount effective to treat a viral, parasitic, or bacterial infection a compound of Formula I; and a method of preparing a compound of Formula I as described herein.
CN102793679A Roxatidine acetate hydrochloride freeze-dried powder injection as well as preparation method and applications thereof The invention relates to a roxatidine acetate hydrochloride freeze-dried powder injection and a preparation method thereof. According to the freeze-dried powder injection, roxatidine acetate hydrochloride is taken as a main drug, a carrier acceptable on pharmacy is selected from any one of the combination of glycine and glutamic acid, the combination of glycine and aspartic acid, the combination of glycine and tartaric acid and the combination of glycine, glutamic acid and aspartic acid, wherein the pH value of the freeze-dried powder injection is 3.5-4.5. According to the freeze-dried powder injection provided by the invention, the hydrolysis reaction of the roxatidine acetate hydrochloride in preparation process is inhibited effectively, the retention period of the freeze-dried powder injection is prolonged obviously, and the stability, safety and effectiveness of the freeze-dried powder injection are improved obviously.
CN103622992A Application of hydrogen sulfide and donor thereof sodium hydrosulfide to preparation of medicament for treating diabetes The invention belongs to the field of pharmacy, relates to novel medicinal application of hydrogen sulfide and a donor thereof sodium hydrosulfide to pharmacy, and in particular relates to application of hydrogen sulfide and donor thereof sodium hydrosulfide to preparation of medicament for treating diabetes. The invention adopts the exogenous hydrogen sulfide and its donor sodium hydrosulfide (NaHS) for insulin sensibilization and tests for regulating blood sugar level and increasing insulin level for type II diabetes. Through correlation test of skeletal muscle and adipose cells with insulin resistance, insulin tolerance test by using animal model for diabetes insulin resistance, glucose consumption experiment, animal model experiment for diabetes insulin resistance and NaHS intervention animal experiment, the results show that NaHS can promote glucose uptake in the presence of insulin, thus indicating insulin enhancement effect. The invention of hydrogen sulfide and the donor thereof sodium hydrosulfide can be used as insulin sensitizers and medicaments for regulating blood sugar level and increasing insulin level for type II diabetes.
CN101376651A Andrographolide and water-soluble aminoacid ester derivative of dewatered andrographolide The invention aims to provide derivatives of amino-acid esters of andrographolidume and dehydrated andrographolidume shown as formulae Ia and Ib. In Ia and Ib, R1, R2 and R3 are H, and the residue of amino acid such as acyl, L-alanyl, L-leucyl, L-valyl or L-isoleucyl; in Ia, R1, R2 and R3 cannot be H at the same time; and in Ib, R2 and R3 can not be H at the same time.
CN103356572A Application of Sarcaboside B in preparation of medicines for treating osteoporosis caused by antiestrogen deficiency The invention discloses a new application of Sarcaboside B for preventing and treating osteoporosis. The osteoporosis is one of major diseases which harm human health, and osteoporosis patients are increasing with the aging of the population, thus enormous social, medical and economic burden is brought in the whole word. Although relevant experts and scholars at home and abroad attach great importance to the osteoporosis, effective medicines for treating the osteoporosis are scare. In-vivo tests prove that the Sarcaboside B has an obvious effect of resting the osteoporosis. Experimental results show that the Sarcaboside B can be used for inhibiting the increasing of the bone conversion rate caused by ovariectomy and the destruction of bones, meanwhile can be used for increasing the concentration of blood calcium and is beneficial to the deposition of bones. The Sarcaboside B has a therapeutical effect on the osteoporosis caused by the antiestrogen deficiency and has no estrogen-like side effect.
WO2010068480A1 Deuterated derivatives of dimeboline This invention relates to novel tetrahydro-lH-pyrido[4,3-b]indoles, their derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by NMDA antagonists, acetylcholinesterase inhibitors, 5-HT6 antagonists, other neuroprotectors, antihistamines and agents that delay age-related pathologies and conditions.
US20120122957 Regulation of aging by modulation of mitochondrial function The invention relates to the field of longevity enhancement. More particularly, the invention provides compositions and methods relating to modulation of mitochondrial function. In certain embodiments, the invention provides methods and related compositions for the enhancement of longevity in an animal, comprising inhibition of one or more electron transport chain components, such as cco-1 and homologs thereof, in a tissue-specific manner in the animal.
CN1823823A medicine and food dual purpose vitamin microelement nutritive product for preventing and treating synchysis and its manufacturing method A nutrient used as both medicine and food for preventing and treating synchysis is prepared from vitamins and trace elements. Its preparing process is also disclosed.
WO2011044540A1 Topical formulation comprising etoricoxib and a zwitterionic surfactant The present invention provides topical pharmaceutical compositions, methods for preparation, and methods of treatment comprising a selective COX-2 inhibitor and useful for the treatment of pain, particularly pain associated with osteoarthritis. The compositions can provide good selective COX-2 inhibitor permeability and bioavailability at the target site. In certain preferred embodiments, the invention provides a pharmaceutical composition comprising etoricoxib, a zwitterionic surfactant or charged derivative thereof, an alpha-hydroxy acid, at least one molecular penetration enhancer, at least one lower alcohol, and water.
WO2006016828A8 Use of alpha ketoglutarate for treating alzheimer, parkinson The invention relates to the use of at least one member selected from the group consisting of alpha-ketoglutarate and its salts: ornithyno-alpha-keto-glutarate, asparagine-alpha-keto-glutarate and other salts with amino acids and salts of alpha-keto-glutarate with metal ions such Na, Ca, Mg, Cu, Sr, Zn, K and others in doses 0.001-1 g/kg/day or in concentration 0.001 mM-100mM for the manufacture of a pharmaceutical preparation and/or food/ feed additive augmenting, supporting the function of the nerve cells and nervous system and simultaneously minimizing, preventing the apoptosis of nerve cells and preventing the development of diseases of nervous system in adolescent, adult and fetuses in mammals, including people, such as Alzheimer, Parkinson, Huntington, Creutzweld-Jakob, BSE and other diseases and protecting the nervous system function against its degeneration due to apoptosis of nerve cells in Alzheimer, Parkinson, Huntington, Creutzweld-Jakob, BSE and other diseases and protecting the growth and stimulating the reproduction and preventing the apoptosis of nerve and other cells in vitro and in biotechnological processes with the use of somatic and bacterial cells .
WO2014015137A3 Compositions and methods for treating dysproliferative diseases Methods are provided for treating cancer and other dysproliferative diseases by administering to a subject in need there of a therapeutically effective amount of a synergistic composition comprising an HER2 inhibitor, or a pharmaceutically acceptable salt or prodrug thereof; and a CYP26 inhibitor, or a pharmaceutically acceptable salt or prodrug thereof; wherein said therapeutically effective amount suppresses the growth of dysproliferative cells in vivo. Compositions comprising a combination of an HER2 inhibitor, or a pharmaceutically acceptable salt or prodrug thereof; and a CYP26 inhibitor a pharmaceutically acceptable salt or prodrug thereof are also described.
WO2011131596A1 Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes as vasopressin v1a receptor antagonists The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula (I) wherein R1, R2 and R 3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in particular as Via receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
WO2008061968A1 Benzimidazolone derivates in the treatment of pulmonary arterial hypertension The invention relates to the use of benzimidazolone derivatives of formula (I) for preparing a medicament for treating diseases in which the use of therapeutic effective amounts of compounds displaying affinity for the 5-HT2B-receptor display a therapeutic benefit.
US20080085306 Topiramate compositions and methods of enhancing its bioavailability The present invention is directed to pharmaceutical compositions that allow for once-daily or alternate day dosage forms of topiramate. The proposed delayed/extended release single dosage form is equivalent to the immediate-release multiple dose daily regimen, and upon administration, provides steady state blood levels of topiramate. Formulations with increased bioavailability and improved pharmacokinetics are disclosed. A once-a-day administration of topiramate is advantageous over the multiple dose regimen both in terms of patient compliance and reduced adverse events, thus providing better treatment of the conditions for which the topiramate is indicated.
CN102145109B Medicament for treating hyperpyretic swine fever and preparation method thereof The invention relates to a medicament for treating hyperpyretic swine fever, which comprises the following components in parts by weight: 1000-3000 parts of fresh artemisia santonica, 750-2000 parts of fresh mugwort, 200-300 parts of garlic clove, 1500-6000 parts of fresh banana tree sap and 300-500 parts of white sugar. The medicament for treating hyperpyretic swine fever, which is provided by the invention, has the advantages of good effect, low cost and high effect taking speed and is safe to use.
CA2853784A1 Treatment of blood lipid abnormalities and other conditions There is provided a method of treatment of a patient suffering from blood lipid abnormality comprises the administration of a GPR119 agonist.
WO2014161872A1 Compositions for use in stimulating bone growth The present invention relates to use of a composition for maintenance of bone and/or cartilage health or prevention, alleviation and/or treatment of bone and/or cartilage disorders.
CN102579390A Ibuprofen timing release three-layer tablet drug composition and method for preparing same The invention relates to the technical field of drug form structures, in particular to an Ibuprofen timing release three-layer tablet drug composition and a method for preparing the same, wherein an Ibuprofen timing release three-layer tablet consists of an Ibuprofen release layer, a coated isolating layer and a coated Ibuprofen release layer, through a large number of tests and prescription screening, the Ibuprofen timing release three-layer tablet is provided for patients, so the domestic blank is filled up, and clinic medicine requirements are satisfied.
CN103301152A Inverted sugar electrolyte injection and preparation method thereof The invention provides inverted sugar electrolyte injection. 1000ml of inverted sugar electrolyte injection comprises the following components by weight: 25-50g of glucose, 25-50g of fructose, 0.73-1.46g of sodium chloride, 0.93-1.86g of potassium chloride, 1.40-2.80g of sodium lactate, 0.375-0.75g of sodium dihydrogen phosphate, and 0.143-0.286g of magnesium chloride. Total parenteral nutritional injection is compounded of electrolyte and inverted sugar; a plurality of electrolytes, glucose and fructose can be simultaneously provided for an organism; and the targets of supplying body liquid to the organism, maintaining water and electrolyte balance and supplying energy are achieved; fussy preparation is reduced; secondary pollution is avoided; and the inverted sugar electrolyte injection has greater clinical application value. The invention provides a preparation method, which is suitable for industrial production.
CN103214478A Pyridineoxopyridazine derivatives The invention belongs to the technical field of medicines, and concretely relates to pyridineoxopyridazine derivatives having structures represented by general formula (I), and pharmaceutically acceptable salts, stereoisomers or solvates thereof. In the general formula (I), R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R<8>, R<9>, R<7'>, R<8'>, R<9'>, L and ring A are defined in the specification. The invention also relates to preparation methods of the above compounds, medicinal compositions containing the compounds, and applications of the compounds and the medicinal components in the preparation of medicines for treating and/or preventing inflammatory diseases, illnesses and patients' conditions characterized by undesired inflammatory immune responses or related with the undesired inflammatory immune responses, and all diseases induced by the hypersecretion of TNF-alpha and PDE-4 or related with the hypersecretion of TNF-alpha and PDE-4.
WO2013058344A1 Method for predicting effect of plk1 inhibitor Provided is a predictable biomarker which is provided for the purpose of predicting the response to a PLK1 inhibitor more accurately and maximizing the benefit of a patient, and which is more specific and can be used in clinical applications. A method for predicting the effect of a PLK1 inhibitor, comprising (1) a step of determining the number of copies of CDKN2A gene in a biological sample from a patient or the nucleotide sequence for the CDKN2A gene; and (2) a step of predicting that the PLK1 inhibitor is effective when the number of the copies is 1 or more, when the determined nucleotide sequence has no mutation, or when a protein encoded by the sequence retains the function of the CDKN2A protein.
CN1876634A Sinomenine structure-modified compound and its preparation method The invention discloses the compound reformed by sinomenine structure and preparing method. The method uses sinomenine as raw material, and carries out chemosynthesis, comprising new substitutive derivative on a ring, B ring, C ring and D ring. The invention has the active in anti-inflammatory, immunity, ease pain and allergic reaction.
CN102441158A Eye drop having Cecropins for pet and preparation method thereof The invention relates to a novel eye drop used for pet. The main ingredients of the eye drop comprise a Cecropins antibacterial peptide, a water-soluble chitosan and a borneol. Apart from the broad-spectrum antibacterial activity, the eye drop also has the resistance effect for virus, parasite, fungus and cancer cell which can enhance the immunity and facilitate the wound healing with no resistance to drugs and no residues after long-term usage. Moreover, the water-soluble chitosan is very excellent in viscosity, mould integration property, antibacterial activity and absorbability, which can overcome the deficiencies of conventional eye drops such easy lose and frequent dose.
CN103006678A Application of houttuynoid A in preparing medicament for treating alzheimer disease The invention discloses an application of houttuynoid A in preparing a medicament for treating alzheimer disease. Houttuynoid A has acetylcholin esterase inhibiting activity and nerve cell protecting effect, and can be used for preparing a medicament for treating alzheimer disease when serving as a multi-target compound. The application of houttuynoid A in preparing a medicament for treating alzheimer disease belongs to first disclosure, which has prominent substantial characteristics because the frame model belongs to a brand-new frame model, and has unexpectedly strong inhibiting activity to acetylcholin esterase without the possibility of giving any revelation by other compounds, and the prevention and treatment of houttuynoid A for alzheimer disease has a remarkable progress.
CN101874784A Crystal separating drug sustained-release microspherule and preparation method thereof The invention discloses a crystal separating drug sustained-release microspherule comprising the following components in parts by weight: 4-9 parts of water-insoluble drug, 0.1-2 parts of sustained-release polymer and 1-4 parts of microspherule bridging agent. In addition, the invention also discloses a preparation method of the crystal separating drug sustained-release microspherule, comprising the following steps: 1) dissolving water-insoluble drug into good solvent to form drug solution; 2) adding the drug solution into the opposite phase solvent of the drug, and stirring; 3) after the injectable suspension of drug microcrystal in the opposite phase solvent is completely formed and stabilized, adding solution containing the sustained-release polymer, the microspherule bridging agent and the solvent, and stirring; and 4) after the drug microspherule is completely formed and the solvent for dissolving the sustained-release polymer and the microspherule bridging agent is completely volatilized, stopping stirring, and filtering and drying the drug microspherule. The method can obtain the granule diameter with wider range, more regular and smooth surface and more controllable inner and outer releasing rate of drug.
US7524881 High purity material from reverse phase column chromatography separation Δ9 THC acid is obtained from plant material and extracted into an aqueous solvent under conditions of pH control. The acid is converted to a salt and the salt extracted into a polar solvent, yielding acid of high purity. The Δ9 THC acid is then converted to Δ9 THC which is further purified and combined with a carrier for pharmaceutical use.
EP1550655A1 Bicyclic intermediates A compound having the following general fomula: wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR4, NR4, O or S in which R4 is H or an optionally substituted hydrocarbon group; R5 is H, a halogen atom, C1-6 alkyl group, a C1-6 alkoxy group, a hydroxy group, a nitro group, a cyano group or an amino group wherein the C1-6 alkyl group, the C1-6 alkoxy group and the amino group may be substituted by 1 to 5 substituents, Y is C or N; ring B is an optionally substituted benzene ring; m = 1 to 4 and n = 0 to 2; L represents a leaving group such as a halogen atom, an alkylsulfonyl group, an alkylsulfonlyoxy group and arylsulfonyloxy group; or a salt thereof.
CN101889992A Application of 2,4-dihydroxy benaophenonel in preparing medicament for treating hepatitis The invention discloses application of a 2,4-dihydroxy benaophenonel in preparing a medicament for treating hepatitis. Virus b hepatitis, cocaine toxic hepatitis, carbon tetrachloride toxic hepatitis, paracetamol toxic hepatitis and thioacetamide toxic hepatitis can be effectively treated by medicaments with the 2,4-dihydroxy benaophenonel as an active ingredient.
US20100190859 Monorasagiline citrate; salt formation; monoamine oxidase inhibitors; side effects reduction; carriers; tablets; transdermal patches; Parkinson's disease; brain disorders; nervous system disorders; neurodegenerative disease; multiple sclerosis The subject invention provides rasagiline citrate, its compositions and processes for the manufacture thereof.
EP0788798B1 Antiviral agent and process for preparing the same A process for preparing an antiviral agent that can inhibit the growth of viruses, is efficacious against retroviruses, does not adversely affect humans, domestic animals and so forth, and has preventive effects, which comprises extracting pecan nuts, pine seeds, Chinese gutta percha (Eucommia ulmoides Oliv., barks), tea prepared therefrom (leaves and twigs), mangrove, balsam pear, or Aspalathus linearis (family Fabaceae) with an alkali, adding ethanol to the obtained extract in a final ethanol concentration of 25 to 75 %, and centrifuging the resultant solution.
WO2011033225A2 Substituted 3-amino-cinnolin-4(1h)-one derivatives, preparation thereof, and therapeutic use thereof The present invention relates to compounds having Formula (I): - R1 is a hydrogen atom or a (C1-C4)alkyl; - R2 is a substituted or unsubstituted (C1-C10)alkyl or a substituted or unsubstituted (C3-C12) non-aromatic carbocyclic radical; - or R1 and R2 together, with the nitrogen atom to which they are linked, form a heterocyclic radical selected from among azetidin-1-yl, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl, and piperazin-1-yl, said heterocyclic radical being substituted or unsubstituted; - R3 is a -(CH2)n-R5 group; - R4 is a hydrogen atom, a halogen atom, an Alk group, or an OAlk group; - R5 is a halogen atom, a CF3 group, or a group selected from among -S-Alk,, -SO-Alk, -SO2-Alk, -N(R6)SO2-Alk; -R6 is a hydrogen atom or a (C1-C4)alkyl; - Alk is a substituted or unsubstituted (C1-C4)alkyl; n is equal to an integer between 2 and 5. The invention also relates to a preparation method and to therapeutic use.
WO2011017456A2 Localized delivery of nanoparticles for therapeutic and diagnostic applications The present invention is directed to compositions and methods of localized delivery of a functionalized nanoparticle.
CN102961594A Foot liquid for treating tinea pedis The invention discloses foot liquid for treating tinea pedis. The foot liquid for treating the tinea pedis consists of the following components in parts by weight: 6 to 9 parts of pawpaw, 1 to 2 parts of solomonseal rhizome, 0.5 to 1 part of rhubarb, 3 to 7 parts of clove, 1.5 to 3.5 parts of alum, 1.2 to 3.5 parts of root bark of shaggy-fruited dittany, 0.8 to 1.25 parts of fistular onion stalk, and the balance of water. The foot liquid has the effects of cleaning, health care, bacteriostasis and sterilization, is convenient to use, and can clear heat and dampness, detoxify, kill worms and effectively treat the tinea pedis.
CN101317877A Far-infrared ray scaly tetter ointment and preparation method thereof The present invention relates to a far infrared ray psoriasis ointment and the preparation method, which can effectively cure the psoriasis. The present invention has the technical proposal that: 1. the far infrared ray psoriasis ointment is characterized in that: the far infrared ray psoriasis ointment comprises 1 to 5 proportions of far infrared ray powder, 35 to 45 proportions of croton fine powder, and 50 to 64 proportions of polyethylene glycol in weight proportion. 2. the preparation method for far infrared ray alphos ointment is characterized in that: the croton is made into coarse powder after the shell is removed. The coarse powder is milled into fine powder after being extracted in carbon dioxide and the oil in the croton is removed. The fine powder is mixed with the far infrared ray powder; the ointment is produced after polyethylene glycol is put into the fine powder mixed with the far infrared ray powder.
CN1927206A Lornoxicam composition for injection and preparation process thereof The invention provides a lornoxicam injection combination, including injection and freeze-dried powder. The combinations contain 0.86-4.3 weight portion of lornoxicam and pharmaceutically acceptable basic amino acids, and the weight rate of lornoxicam and basic amino acids is 1:0.5-20, the present invention also provides corresponding preparation methods. The said combination has good solubility in solution, high stability and it improves the convenience and safety of clinical use.
US7033616 Extracts, compounds and pharmaceutical compositions having anti-diabetic activity and their use The invention relates inter alia to pharmaceutical compositions containing an extract obtainable from a plant of the genus Trichocaulon or Hoodia having anti-diabetic activity; and to the use of such extracts and to compound (1) as herein defined and its analogues for the manufacture of medicaments having anti-diabetic activity.
US20090227636 substituted pyrrolidine derivatives, used for the treatment vision defects such as glaucoma or ocular hypertension Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
WO2010071866A2 Combination therapy for arthritis with tranilast Combination therapy is disclosed herein for the treatment an arthritic condition (e.g. rheumatoid arthritis, osteoarthritis or psoriatic arthritis). The therapies disclosed herein comprise administering tranilast or an analogous compound in combination with a pharmaceutical agent, such as a non-steroidal anti-inflammatory drug, a disease-modifying drug, a COX -2 inhibitor, an antibiotic, an analgesic or combination thereof.
CN100998562A Preparation of vinorelbine lipoplast, for injection A process for preparing the vinorelbine liposome for injection, especially the vinorelbine liposome tartrate, includes such steps as dissolving multiple kinds of lipoid in organic solvent, mixing it with buffer liquid in HPLC gradient pump while pressing, ultrafiltering to remove organic solvent and obtain simple liposome, regulating pH=7-9 by special alkali solution, mixing with medicine solution, and encapsulating to obtain medicine.
US20090104212 Methods and systems for treating cell proliferation disorders using two-photon simultaneous absorption A method for treating a cell proliferation disorder in a subject, comprising: (1) administering to the subject at least one activatable pharmaceutical agent that is capable of activation by a simultaneous two photon absorption event and of effecting a predetermined cellular change when activated; and (2) applying an initiation energy from an initiation energy source to the subject, wherein the initiation energy is capable of penetrating completely through the subject, and wherein the applied initiation energy activates the activatable agent by the simultaneous two photon absorption event in situ, thus causing the predetermined cellular change to occur, wherein the predetermined cellular change treats the cell proliferation related disorder, and a kit for performing the method, a computer implemented system for performing the method, a pharmaceutical composition useful in the method and a method for causing an autovaccine effect in a subject using the method.
US6903115 Bipiperidine compounds The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
WO2007041951A1 Extraction method of abalone polysaccharide An extraction method of abalone polysaccharide characterized in that abalone meat (including organs) is obtained by removing abalone shell, broken the wall with a tissue mincer, uniformly mixed with water, extracted at 20 to 80 °C for 2 to 6h, and separated by centrifugation, the insoluble substance is repeatedly extracted for 1 to 2 times by again adding water, and the supernatant is combined. The extract is concentrated to saccharide content of 1.5 to 3.0 percent, precipitated at 0 to 4 °C for 12 to 16h by adding 3 to 4 times volume of 95 percent ethanol, centrifuged and dried by means of vacuum drying or spray drying to give product. The uniform abalone polysaccharide is obtained by purification with Sephadex G-100 or DEAE-Cellulose after removing protein and glucogen. The extraction can also be preformed by alkali extraction, ultrasonic extraction or enzymic extraction. The enzyme extraction can be preformed with a single enzyme, two enzymes, a complex enzyme or the combination thereof. The enzyme used is pepsin, trypsase and so on. There is provided a process of extracting abalone polysaccharide from abalone (especially from abdominal feet and organs thereof), and therefore abalone polysaccharide extraction and separation can be efficiently preformed. There is provided a technical basis for further research due to continuous intensive research on pharmaceutic use of abalone polysaccharide.
US20120108624 Treatment of dyskinesia related disorders Disclosed herein are methods of treating Parkinsons disease while maintaining a low dyskinesia induction profile and methods of reversing dyskinesias comprising administering a therapeutically effective amount of a compound of the invention. The present invention further relates to uses and pharmaceutical compositions of said compounds in the manufacture of medicaments in treating the same.
EP2392574B1 Indolyl pyrrolidines for the treatment of cancer The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention. where U is:
CN103127063A Application of chloranthus japonicus alcohol F in preparation of antitumor drugs The invention belongs to the chemical field and medical field, and relates to application of chloranthus japonicus alcohol F in preparation of antitumor drugs. Cancer cells comprise hepatoma carcinoma cells and pancreatic cancer cells. The chloranthus japonicus alcohol F belongs to natural products, is small in toxic and side effects, high in bioavailability, and stable in properties, and has clinical value. Small molecule compounds can be used as new antitumor drugs or auxiliary components of the new antitumor drugs to develop, and are obvious in tumor suppression effects, green, and environment-friendly, and provides a new way and method for treating and curing tumours.
US20120148695 Pharmaceutical Compositions From Carapa Guianensis The invention refers to pharmaceutical compositions based on oil extracted from the seeds of Carapa Guianensis Aublet and/or of chemical compounds isolated from this oil and responsible for its biological activity, the tetranortriterpenoids, presenting the following pharmacological activities: anti-allergenic, anti-inflammatory, analgesic and immune modulating with reduced side effects and low cost. Such pharmaceutical compositions of this invention are aimed at the treatment, or prevention, or inhibition of allergenic an inflammatory conditions in human beings, through oral or topic use. In each one of these cases, the composition can be in the liquid or solid form. Compounds for topic use of this invention are atoxic, or with low toxicity, and, specially, provided in the semi-solid form (cream). The pharmaceutical compositions of this invention constitute an important therapeutic alternative for cutaneous and respiratory allergies, besides acting in different inflammatory reactions of allergenic origin or infectious origin. Therefore, these compositions are also used in the symptomatic treatment of rheumatic, inflammatory and degenerative processes, diverse traumas, pain and post surgery inflammation, acute painful syndromes, among others and it can be orally or topically administered.
WO2010053606A3 Small-molecule inhibitors of protein synthesis inactivating toxins Small-molecule inhibitors of a protein synthesis inhibiting toxin, e.g., ricin, abrin, Shiga, and Shiga-like toxins, as well as methods of using the inhibitors are provided. Further provided are methods of identifying small-molecule inhibitors of a protein synthesis inhibiting toxin.
CN1582907A Pseudoephetonin drops and their preparation A dripping pill of pseudoephedrine hydrochloride is prepared by ultrafine pulverizing and conventional process for preparing dripping pills.
US20120028993 Compounds Effective Against Cancer The present invention describes a Composition, comprising one or more compounds selected from the group consisting of a) compound (I) which is ethacrynic acid bezafibrate, fenofibrate, and/or griseofulvin, b) compound (II), which is ciclopirox ciclopirox olamine, octopirox, and/or cinnarizine, c) mixtures of compound (I) and compound (II), or pharmaceutically acceptable derivatives thereof for the treatment of cancer. The present invention is further directed to the use of said compounds or a mixture of compounds for the manufacture of a medicament for the treatment of cancer and to the use of said compound in a method for treating cancers in animals and humans.
EP2603496A1 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
US20090048293 Methods for treating bacillus infection The present invention provides compositions and methods for detecting, treating, and preventing microbial infection, especially infection caused by Bacillus anthracis (“anthrax”).
US7119113 optionally halogenated N-(trifluoromethyloxazol-2-yl)xanthene-9-carboxamides; treatment of neurological disorders such as Alzheimer's disease and dementia The invention relates to carboxamide derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as mGluR1 enhancers in the treatment and prevention of neurological disorders and diseases, such as Alzheimer's disease and dementia.
CN101704795A Hydrochloric acid 2-(1-ethyl propyl) moroxydine, preparation method and application thereof The invention provides a new hydrochloric acid 2-(1-ethyl propyl) moroxydine which can be obtained by chemical synthesis and has the advantages of low price of needed raw materials, easily obtained raw materials, simple and convenient preparation method, higher yield and suitability for industrialized production. The pharmacological activity experiment proves that compared with hydrochloric acid moroxydine, the hydrochloric acid 2-(1-ethyl propyl) moroxydine has the remarkably enhanced activity of in vivo resisting hepatitis B virus, hepatitis C virus, influenza virus, pneumovirus and herpes simplex virus, and the toxicity is one time lower than that of the hydrochloric acid moroxydine. Therefore, the new hydrochloric acid 2-(1-ethyl propyl) moroxydine can be applied to prepare antiviral drugs, especially anti-flu drugs, hepatitis C resisting drugs, hepatitis B resisting drugs, pneumovirus resisting drugs and herpes simplex viral keratitis resisting drugs.
EP1698329A1 Drug-containing nanoparticle, process for producing the same and parenterally administered preparation from the nanoparticle To provide an external preparation or injectable preparation that exerts the effect of enabling transdermal or transmucosal in vivo absorption of fat-soluble drugs and water-soluble drugs not having been satisfactorily attained hitherto and that contains a highly absorbable fat-soluble/water-soluble drug, the injectable preparation especially aiming at sustained-release and target effects. In particular, drug-containing nanoparticles (secondary nanoparticles) are provided by causing primary nanoparticles containing a fat-soluble drug or fat-solubilized water-soluble drug to act with a bivalent or trivalent metal salt. Further, drug-containing nanoparticles (tertiary nanoparticles) are provided by first causing primary nanoparticles containing a fat-soluble drug or fat-solubilized water-soluble drug to act with a bivalent or trivalent metal salt to thereby obtain secondary nanoparticles and thereafter causing a monovalent to trivalent basic salt to act on the secondary nanoparticles. Still further, there are provided a process for producing these nanoparticles, and a transdermal or transmucosal external preparation or injectable preparation in which these nanoparticles are contained.
US20070185071 a compound containing cyclic tetrapeptide coupled to amide, ester, ketone groups; apoptosis and cell differentiation inducer; cancer metastasis and angiogenesis inhibitor; catalytic hydrogenation, acid treatment, fluoride anion treatment, or hydrolysis for deblocking; coupling cyclic tertrapeptide HDAC inhibitors represented by formula (1) show strong inhibitory activity against various subtypes of HDACs. The compounds of the present invention find utility as pharmaceutical agents for treating or preventing diseases associated with HDAC 1, 4, and 6. The methods for producing the compounds of the present invention enable easy and simple synthesis of various types of these compounds, and are expected to contribute to the development of HDAC inhibitors having novel properties and the like.
EP2202241A2 Therapeutic compounds and methods for modulating V3, a versican isoform A method of increasing elastic fibers in human tissue comprises contacting the tissue ex vivo with an effective amount of an agent, wherein the agent increases the amount or activity of versican v3 in said tissue.
WO2009013333A1 Alkylacetylene substituted acyltryptophanols The present invention relates to acyltryptophanols of the general formula (I) in which R1, R2, R3, Q and X have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
US20100074881 Multiple nebulizer systems A device for administering two or more therapeutic agents simultaneously, comprising two or more nebulizers and a single connector linking the nebulizers to a nebulizer mouthpiece. Also provided is a method of administering two or more therapeutic agents simultaneously, comprising administering the therapeutic agents simultaneously with the device of the present invention to a subject in need thereof.
CN1657617A Clone, expression and anti-tick immanoprotection action of falcate rhipicephalus RhcA and RhcB genes The sequences of falcate rhipicephalus RhCA and RhcB genes, the cloning of said RhoA and RhcB genes, their expression in colibacillus, and their anti-tick immunoprotection action to rabbit are disclosed. The present invention provides the basis for preparing anti-tick vaccine and medicine from cysteine proteinase moleculae.
US20090104171 Metabolic Enhancement Therapy A Metabolic Enhancement Therapy nutritional supplement for treating symptoms and conditions such as acute anxiety, hyperactivity, panic attacks, confusion, involuntary movements, sleep disorders, mood disorders, depression, anger, seizures, obsessive-compulsive behavior, unregulated fear, panic, neuronal disorders, autism, schizophrenia, attention deficit disorder (ADD), attention deficit hyperactive disorder (ADHD) and neuronally based immunologic disorders by administering to a mammal an effective amount of acetyl-L-carnitine, α-lipoic acid, biotin, vitamin B1, L-glutamine, Vitamin B6, taurine, folinic acid, vitamin B12, trimethylglycine, and L-tryptophan.
WO2009050201A2 4-phenyl-5-oxo-imidazole derivatives, pharmaceutical compositions and uses therof The invention relates to compound of the formula (I) wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.
CN1251097B Phthalazines with angiogenesis inhibiting activity The invention relates to compounds of formula (I), wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula (I*) or (iii) together form a bridge in subformula (I*), wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, -CH2-O-, -CH2-S-, -CH2-NH-, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfonyl; and wherein the bonds characterized by a wavy line are either single or double bonds; or an N-oxide of said compound with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are as defined, then G is selected from the group comprising lower alkylene, -CH2-O-, -CH2-S-, oxa and thia; or a salt thereof. The compounds inhibit angiogenesis.
US20130035336 Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor for treating cancer A combination of a CDK4/8 inhibitor and an mTOR inhibitor for the treatment of cancer.
US7268160 A therapeutic or prophylactic agent for a disease that requires enhancement of nerve growth factor production, e.g., butein; nervous system disorders; Alzeimher's disease; additive for foods, beverages and feeds The present invention provides a therapeutic agent or prophylactic agent for a disease that requires enhancement of nerve growth factor production, an enhancer for nerve growth factor production, or a food, beverage or feed for enhancing nerve growth factor production, each comprising as an effective ingredient a specified compound or a salt thereof having enhancing activity for nerve growth factor production; a method for enhancing nerve growth factor production, comprising administering to a mammal the above-mentioned compound or a salt thereof; and use of the above-mentioned compound or a salt thereof in the preparation of a therapeutic agent or prophylactic agent for a disease that requires enhancement of nerve growth factor production, an enhancer for nerve growth factor production, or a food, beverage or feed for enhancing nerve growth factor production. In addition, the present invention provides novel compounds having enhancing activity for nerve growth factor production.
WO2009055445A2 RNA INTERFERENCE MEDIATED INHIBITION OF RESPIRATORY SYNCYTIAL VIRUS (RSV) EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) Compounds, compositions, and methods for mediating RNA interference (RNAi) against respiratory syncytial virus (RSV) gene expression are provided, useful for preventing, inhibiting, or reducing RSV infection, liver failure, hepatocellular carcinoma, cirrhosis, and/or other disease states associated with RSV infection in a subject or organism.
WO2009119710A1 Novel antibiotic sf2896 substance, process for production thereof, and pharmaceutical composition Disclosed are a novel antibacterial agent and a process for the production thereof. Disclosed are: a novel thiopeptide compound produced by an actinomycete belonging to the genus Nonomuraea, i.e., a compound represented by formula (1) or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising the compound or the pharmacologically acceptable salt thereof as an active ingredient; and a process for producing the compound.
WO2005115426A1 Drug for ameliorating male climacteric disorder It is intended to provide a drug or a food with a high safety which inhibits a decrease in the blood testosterone level and thus prevents or ameliorates symptoms associating male climacteric disorder. Namely, a blood testosterone level lowering inhibitor or a drug for ameliorating male climacteric disorder which contains a plant belonging to the genus Codonopsis or its extract.
WO2008058438A1 The use of ferric citrate in the manufacture of medicaments for treating blood vessel calcification The use of ferric citrate in the manufacture of medicaments for treating blood vessel calcification comprising cardiovascular heterotopic calcification. The therapeutic effect thereof is definite. It is shown in the tests that ferric citrate can inhibit effectively calcification and may reverse occurrence of calcification by interfering the process of calcification.
US7329661 N-phenyl-3-pyrimidine-amine derivatives The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.
CN101856324A Method for preparing phloroglucinol injection The invention belongs to the field of medicinal preparations, and discloses a method for preparing phloroglucinol injection. The method for preparing the phloroglucinol injection comprises the following steps of: (1) preparing solution containing phloroglucinol and trimethyl phloroglucinol; (2) stirring the solution uniformly and then filtering the solution for sterilization; (3) encapsulating the filtered solution by a conventional method and sterilizing the encapsulated solution, wherein the temperature for the sterilizing filtration in the step (2) is 5 to 40 DEG C, and preferably 10 to 35 DEG C. The technical scheme can ensure stable content of the trimethyl phloroglucinol during the preparation of the phloroglucinol injection. Meanwhile, the method for preparing the phloroglucinol injection ensures the sterility assurance level of the injection by using the sterilization process with over sterilization effect.
WO2009043577A3 Contraceptive 19-nor progesterones The invention relates to compounds of general formula (I), methods for the production thereof, pharmaceutical or cosmetic compositions or forms of administration containing said compounds, and contraceptive methods by administering said compounds.
CA2806450A1 Process for the esterification of hyaluronic acid with hydrophobic organic compounds The invention relates to a process for providing esters of hyaluronic acid, hyaluronic acid salts or hyaluronic acid derivatives with hydrophobic organic compounds. The process includes the steps of (i) micronizing the hyaluronic acid, salt or derivative thereof at reduced temperature, (ii) reacting the hydrophobic compound with a micronized hyaluronic acid obtained in (i) in a suitable solvent; and (iii) filtrating or dialyzing reaction mixture obtained in (ii) to obtain the desired ester. Also encompassed by the present invention are the esters obtained by such a method and compositions containing them as well as the use thereof for treating and/or preventing cartilage damage and inflammation.
CN1800177A Reduced aminate of geniposide huperzine A and its preparation method and uses The invention relates to a structured (I) compound Cape jasmine aglycone Huperzine reduction amination product. It also relates to the method for preparing for the compound and the applied in treating neurological disorder.
US20100303829 Hiv vpr-specific t cell receptors The instant invention provides TCRs having one or more amino acid substitutions that bind to the AL9 epitope of the HIV protein vpr (AIIRILQQL (SEQ ID NO: 1)).
CN102018667A Imidazoles antifungal skin wiping agent and preparation method thereof The invention discloses an imidazoles antifungal skin wiping agent which is characterized by comprising the following materials in percent by weight: 0.1-5% of imidazoles antifungal drug, 1-5% of surface active agent, 2-4% of skin penetrant, 3-5% of drug release agent, 30-50% of water-soluble cosolvent, 3-7% of thickener, 0.5-1% of salts, 0.2-0.5% of antistatic agent, 0.1-0.3% of coloring agent, 0.7-1.5% of nutrition agent and the balance of distilled water. The skin wiping agent has the advantages of little viscosity, stable property and stable releasing speed, can enter blood circulation through the skin and has continuous and strong effect on treating fungoid whelk, scurf and the like caused by fungus. The invention also provides a preparation method of the imidazoles antifungal skin wiping agent.
EP1049700B9 Chemokine receptor antagonists and methods of use therefor Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by structural formula (I) and physiologically acceptable salts thereof.
US20080045520 Substituted Pyrrolidine Derivative The present invention contemplates provision of a quinolone antibacterial agent and a drug for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), and which exhibit higher safety. A compound represented by the following formula (I): a salt of the compound, or a hydrate of the compound or the salt; and an antibacterial drug and an infectious disease treating drug containing the compound as an active ingredient.
WO2008126918A1 Twelve-membered cyclomacrolactam derivative This invention provides a twelve-membered cyclomacrolactam derivative having antitumor activity, more specifically a compound represented by formula (1) or its salt. In formula (1), R1 represents a hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, or a C6-14 arylcarbonyl group; R2 represents a hydrogen atom or a C1-6 alkyl group; R3 represents a hydrogen atom or a hydroxyl group; R4 represents a hydrogen atom or a hydroxyl group; R5 represents a hydrogen atom or a C1-6 alkyl group; R6 represents a hydrogen atom or a hydroxyl group; and R7 represents an acetyl group or the like.
US6875886 Modified PSMA ligands and uses related thereto The instant invention provides reagents and methods for diagnosis, detection and treatment of cancers (for example, prostate cancers). In particular, the invention provides methods to generate various functionalized PSMA ligands, and their uses in diagnosis, detection, imaging, and treatment of prostate cancers, especially those overexpressing PSMA.
CA2607524A1 Agent for prophylaxis and treating of pancreatitis A pharmaceutical composition for preventing and treating pancreatitis comprising as an active ingredient, a 5-HT2A receptor antagonist, characterized in that the binding activity (pKi) of the 5-HT2A receptor antagonist to 5-HT2A receptor is higher by a value of not less than 1.0 than the binding activity to 5-HT2B and 5-HT2C receptors is disclosed. The binding activity (pKi) of the 5-HT2A receptor antagonist to 5-HT2A receptor is preferably 7.0 or higher and more preferably 8.0 or higher. The invention also provides a method of identifying a candidate substance of the agent for preventing/treating pancreatitis comprising measuring whether or not a test substance has a 5-HT2A receptor antagonism.
WO2007113202A1 Piperazine derivatives as growth hormone secretagogue (ghs) receptor agonists The present invention relates to compounds of formula (I), processes for their preparation, pharmaceutical compositions containing the same and to their use in the treatment of gastrointestinal and other disorders.
US20100310648 Pharmaceutical dosage form for oral administration of a bcl 2 family inhibitor The invention relates to a pharmaceutical dosage form which comprises a solid dispersion product comprising N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide or a salt, hydrate or solvate thereof, at least one pharmaceutically acceptable polymer, and at least one pharmaceutically acceptable solubilizer. The invention is further directed to processes for preparing the pharmaceutical dosage form and to use of the dosage form for treating proliferative disorders.
EP1841434A1 Combination therapy for treating heart disease A combination therapy and co-therapy method for administering therapeutic doses of an aldosterone antagonist agent and a metolazone-related compound to a subject in need of treatment for hypertension, congestive heart failure, and chronic kidney disease are provided. A pharmaceutical composition comprising these therapeutic agents is also provided.
CN102048832A Method for preparing refreshing ointment The invention belongs to the fields of fine chemical industry and in particular relates to a method for preparing refreshing ointment. The refreshing ointment is prepared by mixing 1 to 4 weight parts of methyl salicylate, 40 to 60 weight parts of menthol, 10 to 30 weight parts of borneol, 10 to 40 weight parts of aromatic volatile oil and 10 to 30 weight parts of talcpowder uniformly, wherein the aromatic volatile oil is prepared from one or more of atraotydin, patchouli and folium eucalypti. The method for preparing the refreshing ointment is simple in process and low in cost, and the refreshing ointment is unique in odor, high in refreshing speed and durable in effect.
US7365079 2-(2-naphthyl)-4'-[3-oxospiro[6-azaisobenzofuran-1(3H),1-cyclohexan]-4'-yl]-1H-imidazole; metabolic, genitalor reproductive, gastro-intestinal, respiratory system disorders, antiinflammatory agent or glaucoma; cyclization The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
WO2006034341A3 Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
CN103251956A Matrine-montmorillonite nano composite and preparation method thereof The invention provides a matrine-montmorillonite nano composite and a preparation method thereof. The nano compsite comprises matrine and montmorillonite. The interlamellar spacing of the montmorillonite is 1.8-1.86 nm. The preparation method comprises the following steps of: (1) uniformly mixing the montmorillonite with urea, performing solid phase grinding so that the interlamellar spacing of the montmorillonite is enlarged under the action of the urea until a powder body to be ground is sticky and wet, thereby obtaining the montmorillonite treated by the urea; and (2) weighing the matrine, dissolving the matrine in water, adding the matrine into the montmorillonite treated by the urea in batches, then commixing and stirring the matrine and the montmorillonite treated by the urea, centrifuging and collecting precipitates, and drying and grinding the precipitates to obtain the nano composite. The interlamellar spacing of the montmorillonite is enlarged by a solid phase grinding method under the action of the urea; then by the solution commixing method, the montmorillonite can effectively bear the matrine medicines and slowly control the release of the matrine medicines; and the matrine-montmorillonite nano composite is safe and has no toxic and side effect.
WO2011145993A1 Treatment for reducing inflammation A method of treating endometriosis in a person by reducing a cytokine MCP-1 related activity level of an endometriosis implant in said person by 50 % or more while not affecting a corresponding TNF-α related activity level by more than 30 % comprises providing a pharmaceutical composition comprising a local anaesthetic, in particular lidocaine hydrochloride, and a pharmaceutically acceptable carrier, administering the composition intraperitoneally to said person, thereby substantially reducing the recruitment of macrophages by MCP-1 released from the endometriosis implant. Also disclosed is a corresponding pharmaceutical composition.
US20100272783 Methods of Treating Infections of the Nail Disclosed herein are compositions and methods of treating or preventing an infection of the nail, claw, or hoof comprising administering to a subject a pharmaceutical composition comprising an N-halogenated or N,N-dihalogenated amine compound of the application.
CN102367285A Pearsonothuria graeffei fucosylated chondroitin sulfate, extracting method thereof, and purpose thereof The invention discloses pearsonothuria graeffei fucosylated chondroitin sulfate with a structural formula represented as the following. The main chain is in a chondroitin sulfate A structure. The structure also contains a branched chain composed of fucoidan sulfate. The branched chain is connected on a beta-D-glycuronic acid of the main chain through a glucosidic bond. The substitution manners of sulfate groups are 75%3,4-O-SO4, 20%2,4-O-SO4, and 5%4-O-SO4. The invention also discloses an extraction method of pearsonothuria graeffei fucosylated chondroitin sulfate. The polysaccharide provided by the invention provides a function of anticoagulation or antithrombosis.
WO2007010974A1 Use of antihypergycemic effect of d-allose [PROBLEMS] To provide a composition having an effect of preventing the rapid increase in blood glucose level upon the intake of a carbohydrate and/or a sugar. [MEANS FOR SOLVING PROBLEMS] Disclosed is a composition comprising D-allose which can prevent the rapid increase in blood glucose level upon the intake of a carbohydrate and/or a sugar. The D-allose may be a chemical compound D-allose and/or a derivative thereof. Alternatively, the D-allose may be a mixture of D-allose with D-psicose and/or a derivative thereof which is contained at a smaller ratio (by weight) than that of D-allose. Also disclosed is a method for reducing the dietary limitation imposed on a human and/or animal due to abnormal glucose and/or lipid metabolism by using the composition to improve the quality of life (QOL) in the human or animal.
US20120309819 Acid-Labile Lipophilic Prodrugs of Cancer Chemotherapeutic Agents The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.
CN102764437A Methoxsalen injection and preparation method thereof The invention relates to a methoxsalen injection which is prepared through the steps of dissolving a methoxsalen active pharmaceutical ingredient in an organic solvent, adding in propylene glycol, then adding in an isotonic adjusting agent to adjust the isotonicity of the injection, and finally adding in a buffer solution system to adjust the PH of the injection to 3.6-6.0, wherein the buffer solution system is a buffer solution system of sodium acetate and glacial acetic acid, or sodium citrate and citric acid, or disodium hydrogen phosphate and the citric acid. According to the methoxsalen injection and a preparation method thereof, the buffer solution system such as sodium acetate and glacial acetic acid is adopted to adjust the PH to 3.6-6.0, a certain amount of propylene glycol is added to enable the methoxsalen injection to have a good storage stability, especially in 5-day and 10-day experiments at a high temperature, the methoxsalen injection shows a good stability, lactone structures are not hydrolyzed, and each index accords with standards.
CN102204999A Method for measuring content of luteolin in callicarpa nudiflora preparation The invention discloses a method for measuring the content of luteolin in a callicarpa nudiflora preparation, relating to a method for measuring the content of effective ingredients in the callicarpa nudiflora preparation. A high performance liquid chromatography (HPLC) is used for measuring the content of luteolin in the test article solution of the callicarpa nudiflora preparation. Chromatographic conditions and system suitability are as follows: octadecylsilane chemically bonded silica is used as a filler, a flowing phase contains an organic solvent and an acidic solution, the weight percent of the organic solvent in the flowing phase is 50-70%, the weight percent of the acidic solution in the flowing phase is 30-50%, the concentration of the acidic solution is 0-0.3%, and the detection wavelength is 340-355nm. The method disclosed by the invention can be used for accurately and effectively measuring the content of luteolin in the callicarpa nudiflora preparation, has a small error, can further improve the quality standard of the callicarpa nudiflora preparation, and can ensure the quality and clinical effect of the callicarpa nudiflora preparation.
US20120122776 Dpp-iv inhibitors for treatment of diabetes in pediatric patients The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in paediatric patients.
US20120142693 Crystalline compound of 7-[(3r)-3-amino-1-oxo-4-(2, 4, 5-trifluorphenyl)butyl]-5, 6, 7, 8-tetrahydro-3-(tri fluormethyl)-1, 2, 4 -triazolo[4,3-a]pyrazin A crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine (INN: Sitagliptin) of formula 1 with fumaric acid or a hydrate thereof, where the molar ratio of the compound of formula 1 to fumaric acid is 1:0.6 to 1:1.3 is described.
US8461146 Pharmaceutical composition for the treatment of premature ejaculation The present invention provides an oral pharmaceutical composition for the treatment of premature ejaculation, and the composition provides the effective and excellent treatment of premature ejaculation as well as reduced side effects like nausea, vomiting, drowsiness, sedation effect, awakening effect, and weight-loss etc.
US20080249065 glycine and proline; to treat a corneal ulceration; promote corneal re-epithelialisation and rapid healing; treatment of dry eye This invention relates to ophthalmic wound-healing pharmaceutical compositions based on amino acids and sodium hyaluronate.
WO2014064191A3 Drug combinations containing statins for treating cardiovascular diseases The present specification discloses compositions comprising a pharmaceutical composition to reduce or maintain LDL and/or cholesterol levels in an individual and a plurality of therapeutic compounds to increase or maintain HDL levels in an individual. The present specification also discloses a treatment protocol wherein a pharmaceutical composition is administered to an individual on a schedule wherein the pharmaceutical composition is provided for a period of time and then not provided to the individual and this treatment protocol is repeated for the term of the individual's treatment.
US20110251233 Formulation for the buccal transmucosal administration of setrons The invention provides a formulation for transmucosal administration of at least one active ingredient from the setron family, the formulation comprising said active ingredient in base form and/or in salt form, a hydroalcoholic solution titrating at least 30° alcohol, and optionally a pH correcting agent, said active principle being present in the state of stable and complete dissolution in the hydroalcoholic solution. The invention also provides a method of preparing this formulation and its use for the treatment and prevention of major nausea and/or vomiting syndromes, and also for the treatment and prevention of digestive spasms.
WO2008115593A1 1-[(2'-substituted)-piperazin-1'-yl]-isoquinolines as norepinephrine transporter inhibitor therapeutics and positron emission tomography imaging agents Racemic mixtures and enantiomerically pure forms of novel 1-[(2'- substituted)-piperazin-1'-yl]-isoquinolines are norepinephrine (NE) transporter (NET) inhibitor compounds. Compounds of the invention are considered therapeutic agents for central nervous system (CNS) diseases and disorders, without limitation, including neurodegeneration, anxiety, depression, attention deficit disorders, drug dependency, and post traumatic stress disorder. Examples of the chemical syntheses of the compounds of the invention are provided. The isoquinoline compounds of the invention competitively bind at NET at nanomolar concentrations. The isoquinoline agents of the invention bind selectively to NET over other competitive transporter targets and receptor binding sites, including those of serotonin and dopamine, amongst others. The chemical syntheses of the invention are suitable for labeling with radionuclide atoms. Radiolabeled forms of the novel 1-[(2'-substituted)-piperazin-1'- yl]-isoquinoline comoundss are positron emission tomography and single photon emission tomography imaging tracers. Methods of in vivo imaging with the tracers within various subjects and tissues therein, including regions of the brain, are provided. Imaging methods with the tracers in combination other NET inhibitor agents are provided. The imaging methods within subjects allow quantitative detection of NET, determinations of NET distributions, and measures of tracer interactions at NET in the presence or absence of non-radioactive NET agents. The tracer imaging methods are suitable to locate, diagnose, identify, evaluate, detect or quantitate NET, or abnormalities of NET, or NE abnormalities; that are associated with various CNS diseases and disorders.
WO2011006263A8 Antibacterial oral composition The present document describes methods of use of photoactivated compositions for oral disinfection and/or treatments which comprise at least one oxidant, at least one photoactivator capable of activating the oxidant, and at least one healing factor chosen from hyaluronic acid, glucosamine and allantoin, in association with a pharmacologically acceptable carrier.
US20100222383 Iminosugars and methods of treating viral diseases Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.
CN103044338A miR-2 small molecule and application The invention relates to an miR-21 small molecule inhibitor and an application The medicament of the invention can specifically inhibiting the expression of miR-21, thereby promoting a compound 2,4-diamino-1,3-diazacyclohexane-5-nitrile which can induce various tumor cell apoptosis. The binding capability of 2,4-diamino-1,3-diazacyclohexane-5-nitrile is that: Ki=1.49nM, deltaG=-12.04kcal/mol. The preparation method comprises: dissolving 2,4-diamino-1,3-diazacyclohexane-5-nitrile in deionized water to prepare mother solution, adding the mother solution into a tumor cell (colloid tumor, stomach cancer and breast cancer) culturing system according to a certain proportion. The medicament can specifically inhibit the expression of miR-21 without affecting the expression of miRNA. The cell cycle appearances G0/G1 phase arrest, the cell apoptosis proportion is obviously increased, and more effective inhibition to tumour can be implemented.
CN102786468A Nicotinic acid derivative having GK (glucokinase) and PPAR (peroxidase proliferator-activated receptor) dual agonist activities The invention discloses a new nicotinic acid derivative, its preparation method, its medicinal composition and its uses, and concretely relates to an nicotinic acid derivative with the structure represented by general formula I, its medicinal salt, its preparation method, a combination containing one or more of the compound, and uses of the compound in the treatment of diseases associated with the GK and the PPAR, such as diabetes and obesity.
CN103536562A Ambroxol hydrochloride composition freeze-dried powder for injection The invention discloses an ambroxol hydrochloride composition freeze-dried powder for injection, and belongs to the field of medicine and medicine preparation technology. The ambroxol hydrochloride composition freeze-dried powder comprises following raw material ingredients, by weight, 7.56 to 9.67 parts of ambroxol hydrochloride, 5.14 to 6.95 parts of chitosan nanoparticle, and 84.25 to 89.91 parts of injection water. Advantages of the ambroxol hydrochloride composition freeze-dried powder are that: 1) the ambroxol hydrochloride composition freeze-dried powder is capable of eliminating phlegm; 2) the ambroxol hydrochloride composition is capable of improving phlegm eliminating effect of ambroxol hydrochloride greatly, reducing dosage of ambroxol hydrochloride in clinic, and reducing adverse reaction of ambroxol hydrochloride; 3) medicine water solubility is increased, and at the same time, excellent medicine stability is ensured; 4) the nanoparticle medicine carrier is capable of changing membrane transport mechanisms, and increasing medicine permeability against biological membranes, and is beneficial for exhibition of pharmacological functions in cells; and 5) the chitosan nanoparticle can be used as a freeze-dried skeleton agent of the freeze-dried powder injection instead of mannitol so as to avoid active effects of mannitol on human bodies.
US20130035386 Bis[thiohydrazide amide] compounds for treating leukemia Certain bis[thio-hydrazide amide]-related compounds are found to be surprisingly effective at treating with leukemia, e.g., acute myeloid leukemia (AML). Methods of treating a subject with AML including administering bis[thio-hydrazide amide]-related compounds described herein, are disclosed.
CA2658069A1 Medicagenic acid saponin and uses thereof A cholesterol-lowering preparation comprising medicagenic acid saponin is disclosed. The amount of medicagenic acid saponin in the preparation is greater than 50% by weight to produce the cholesterol-lowering effect in an animal. A method of purifying a preparation of at least 30% medicagenic acid saponin is also disclosed. The preparation may be purified from alfalfa plants and used as a treatment for lowering cholesterol and triglycerides in an animal, in particular a human.
CN1839870A Use of geniposide as glicetin 1 acceptor excitomotor The invention discloses the use of geniposide as receptor agonist of glucagon-like peptide-1, which can induce PC12 cell differentiation by means of Mitogen-activated protein kinase (MAPK) to be antagonistic to oxidation injury induced by A beta 25-35. Geniposide can be used for treating nerve retrogression diseases such as AD caused by oxidation injury.
EP2149573A1 Substituted indole sulfonamide compounds their preparation and use as medicaments The present invention relates to indole sulfonamide compounds of general formula (I), a process for their preparation, a medicament comprising these compounds and the use of the indole sulfonamide compounds for the preparation of medicaments for 5-HT6 receptor regulation as well as for the treatment of disorders related thereto.
CN102329285A Epoxy alkynol compound and preparation and use thereof The invention discloses a novel panaxydol compound with optical isomers (3R, 9S, 10S)-9, 10-epoxy-1-heptadecene-4, 6-diyne-3-ol, belonging to the medical technical field. According to pharmacological tests, the compound disclosed by the invention has better anti-tumor activity. The invention additionally discloses a compound synthesis method, which has the advantages of few reaction steps, moderate reaction conditions, high yield, good stereoselectivity and the like.
CN101297888A Medicament composition and preparation thereof The invention discloses a pharmaceutical composition and a preparation method thereof; active ingredients of the pharmaceutical composition comprise membranous milkvetch root, lucid ganoderma, danshen root, white paeony root, tangerine peel, Mongolian dandelion herb, hawthorn fruit, liquoric root, taurine and sodium selenite. The pharmaceutical composition has significant effects on protecting liver and enhancing immunity.
US20110071208 Lipid encapsulated dicer-substrate interfering rna The present invention provides novel, stable nucleic acid-lipid particles comprising one or more Dicer-substrate dsRNAs and/or small hairpin RNAs (shRNAs), methods of making the particles, and methods of delivering and/or administering the particles (e.g., for the treatment of a disease or disorder). In some embodiments, the nucleic acid-lipid particles of the invention comprise Dicer-substrate dsRNAs and/or shRNAs. In other embodiments, the nucleic acid-lipid particles of the invention comprise Dicer-substrate dsRNAs and/or shRNAs in combination with one or more additional interfering RNAs (e.g., siRNA, aiRNA, and/or miRNA). In further embodiments, the Dicer-substrate dsRNAs and/or shRNAs present in the nucleic acid-lipid particles of the invention are chemically synthesized.
WO2005009987A1 Piperidine compounds and pharmaceutical compositions containing them Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In embodiment, the Piperidine Compound has the formula: and pharmaceutically acceptable salts thereof, wherein Ar1, Ar2, X, R3, R4, and m are as disclosed herein.
US7968118 Anti-acid pharmaceutical composition in powder form and process for making it An anti-acid pharmaceutical composition for the rapid and prolonged neutralization of gastric acidity with mucosa-protecting activity in powder form to prepare, by dispersion in water, a pharmaceutical solution or suspension for oral use characterized in that the composition includes sodium alginate; an anti-acid soluble agent or a combination of anti-acids; an inhibitor of proton pump; diluent and sweetening agents, wherein a) at least 30% of sodium alginate present in the formulation along with the total of the inhibitor of proton pump are homogeneously distributed over the surface of the total soluble anti-acid agent of the combination of anti-acids of the composition; and b) the rest, about 70%, of sodium alginate present in the formulation contains a percentage of humidity of less than 2%.
US20090082313 Multikinase Inhibitors for Use in the Treatment of Cancer The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
WO2006028957A8 4-substituted 4, 6-dialkoxy-cinnoline derivatives as phospodiesterase 10 inhibitors for the treatment of psychiatric or neurological syndroms The present disclosure relates generally to the field of phosphodiesterase 10 (PDE10) enzyme inhibition by cinnoline compounds of Formulas: (I) and (II); wherein R'-R3 and R15-R18 are as defined herein. Still further, the present invention provides methods for synthesizing compounds with such activity and selectivity, as well as methods of and corresponding pharmaceutical compositions for treating a patient, e.g., mammals, including humans, in need of PDE inhibition. Treatment is preferably for a disease state that involves elevated intracellular PDE10 levels or decreased cAMP and/or cGMP levels, e.g., involving neurological or psychiatric syndromes, especially those states associated with psychoses, most especially schizophrenia or bipolar disorder, obsessive-compulsive disorder, and/or Parkinson’s disease. In particular, such psychoses, obsessive-compulsive disorder, and/or Parkinson’s disease are due at least in part to catabolism of intracellular cAMP and/or cGMP levels by PDE10 enzymes or where such an impaired condition can be improved by increasing cAMP and/or cGMP levels.
WO2013111013A3 Methods for treating alzheimer's disease by administering certain synthetic compounds Use of a synthetic compound selected from the group consisting of JKF-006, JKF-011 and JKF-027 in the preparation of a medicament for treating Alzheimer's disease.
US20090075909 Derivatives Of Pentose Monosaccharides As Anti-Inflammatory Compounds The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds of this invention can be useful for inhibition and prevention of inflammation and associated pathologies, including inflammatory and autoimmune diseases, for example, bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection or psoriasis. The present invention also relates to pharmacological compositions containing these monosaccharide derivatives, as well as methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, type I diabetes, psoriasis, allograft rejection, and other inflammatory and/or auto immune disorders.
US20120251496 Ezatiostat for treating multiple myeloma Ezatiostat is useful for inhibiting multiple myeloma cell proliferation and treating multiple myeloma, alone or when added together with another anti-myeloma drug.
CN103070821A Method for preparing tulathromycin oral solution The invention relates to a tulathromycin oral solution used for treating animal respiratory diseases, and especially relates to an oral solution used for treating pig respiratory diseases.
EP1147085B1 Alkynyl containing hydroxamic acid derivatives, their preparation and their use as matrix metalloproteinase (mmp) inhibitors / tnf-alpha converting enzyme (tace) inhibitors Compounds of formula (I) wherein R1 is hydrogen, aryl, heteroaryl, alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cycloalkyl of 3-6 carbon atoms, or -C4-C8-cycloheteroalkyl; R2 and R3 are hydrogen, alkyl of 1-6 carbon atoms, -CN, or CCH; R8, R9, R10 and R11 are hydrogen, aryl or heteroaryl, cycloalkyl of 3-6 carbon atoms, -C4-C8-cycloheteroalkyl, alkyl of 1-18 carbon atoms, alkenyl of 2-18 carbon atoms, alkynyl of 2-18 carbon atoms; with the proviso that one of the pairs R8 and R9, R9 and R10 or R10 and R11, together with the carbon atom or atoms to which they are attached, form a cycloalkyl ring of 3-6 carbon atoms, or a -C4-C8-cycloheteroalkyl ring; R12 is hydrogen, aryl or heteroaryl, cycloalkyl of 3-6 carbon atoms; -C4-C8-cycloheteroalkyl, or alkyl of 1-6 carbon atoms; A, X are O, S, SO, SO2, NR7, or CH2; Y is aryl or heteroaryl, with the proviso that A and X are not bonded to adjacent atoms of Y; and n is 0-2; or a pharmaceutically acceptable salt thereof; useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
CN101961318A Lappaconitine sustained release microspheres for injection and preparation method thereof The invention discloses a lappaconitine sustained release microspheres for injection, which is characterized by comprising of lappaconitine accounting for 9.1-50.0% of the weight of the microsphere and biological degradable high polymer material accounting for 90.9-50.0% of the weight of the microsphere, wherein the diameter of the microspheres is 1-250 mu m. The invention has the advantages that (1) the drug entrapment rate is high, the drug loading amount is large, and microsphere distribution is uniform; (2) the drug sustained release period is longer, the release is stable, the burst effect is smaller, and after the microsphere powder prepared by the invention is dispersed in normal saline for muscle or subcutaneous injection, the drug administration frequency can be lowered, therefore, patients are facilitated, patient compliance is improved and the curative effect of the lappaconitine can be improved; (3) the photostability of the lappaconitine can be improved by coating the lappaconitine in the microspheres, and the lappaconitine can be prevented from hydrolysis by preserving the drug loading microspheres in a solid powder form; and (4) the preparation method is simple, the preparation process is and stable and feasible, and the industrial production is easy to realize.
CN101579342A Desloratadine-contained patulin composition The invention relates to a desloratadine-contained patulin composition. The patulin composition contains desloratadine, paracetanol or ibuprofen, pseudoephedrine sulfate or ephedrine hydrochloride and pharmaceutical acceptable auxiliary materials. The desloratadine-contained patulin composition has little sedative effect on the central nervous system, rapid and great effect, long effect duration and little dosage.
WO2013077228A1 Impdh inhibitor having microrna as active component Provided is a novel IMPDH inhibitor based on miRNA. This IMPDH inhibitor has, as an active component, oligonucleotides based more specifically on a miR-19a. The oligonucleotides based on miR-19a comprise a base sequence shown in any of 1) to 5) below: 1) the base sequence represented by sequence number 1 (UGUGCAAAUCUAUGCAAAACUGA); 2) the base sequence represented by sequence number 2 (AGUUUUGCAUAGUUGCACUACA); a base sequence obtained by substitution, deletion, insertion, or addition of one to three nucleotides to a base sequence shown in sequences 1 or 2; base sequences complementary to the base sequences of oligonucleotides shown in any of 1) to 3) above; and base sequences which encode any of the oligonucleotides in 1) to 4) above. The aforementioned oligonucleotides suppress biosynthesis of IMPDH proteins by acting on the mRNA of the IMPDH gene, and can function as an IMPDH inhibitor.
EP2718293A1 Substituted pyridopyrazines as novel syk inhibitors Provided are pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.
US7176189 Methods for regeneration of a mammalian lens The invention relates to methods for transdifferentiation of body tissues which can be used to generate specific cell types needed for regenerating a lens in the mammalian eye, following loss or removal of the original lens.
WO2007146438A1 Hif hydroxylase inhibitors for treatment of anemia of cancer The invention relates to methods and compounds for treating anemia of cancer. In particular, methods for treating anemia of cancer in a subject having cancer, and methods for increasing reticulocytes, increasing hemoglobin, increasing hematocrit, and increasing red blood cell count in subjects having anemia of cancer, wherein such subjects are refractory to treatment with recombinant human erythropoietin (EPO) are encompassed herein.
CN102895185A Bifendate nanosuspension and preparation method and application thereof The invention discloses a bifendate nanosuspension. The bifendate nanosuspension is prepared by mixing bifendate and a stabilizer solution and then grinding by a nano-grinding machine; and a stabilizer is one or more of hydroxypropyl methyl cellulose, hydroxy propyl cellulose, methyl cellulose, polyvinylpyrrolidone, polyethylene glycol, fatty glyceride, a polyol type nonionic surfactant, a polyethylene oxide type nonionic surfactant, poloxamer, tween, tocopheryl polyethylene glycol succinate, phospholipid, gelatin, xanthan gum, sodium dodecyl sulfate and sodium deoxycholate. In addition, the invention also discloses a preparation method for the bifendate nanosuspension and application of the bifendate nanosuspension to a medicinal preparation. The average particle size of the bifendate in the bifendate nanosuspension is less than 1,000nm, so that the solubility of the bifendate is remarkably improved, and the dissolution rate of the bifendate is increased, and the oral bioavailability of the bifendate is improved.
US20070275956 Novel Heterocyclic Compounds Disclosed are novel compounds of formula (I, having hypolipidaemic and hypocholesterolemic properties, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
EP2786747A1 Promoting hair growth solution containing chlorine dioxide preparation method and use method thereof An externally-used solution containing chlorine dioxide for promoting hair growth is composed of chlorine dioxide or its precursors, pH regulators, medical solvents and plant extract in a certain weight ratio. The product may take the forms of a single solution containing chlorine dioxide or several solutions containing a chlorine dioxide precursor. The safety and effective oxidation sterilization and tissue regeneration ability of chlorine dioxide are introduced into the solution system for promoting hair growth, and the steps of removing hair loss factors, stimulating the growth of hair follicles, anti-inflammatory and anti-dandruff are done synchronously. Complemented medical solvents and plant extracts will change alopecia environment.
EP1154999B1 Nitroxyderivatives having antiinflammatory, analgesic and antithrombotic activity Organic or inorganic salts of compounds of general formula: A - X1 - N(O)z for use as medicaments having anti-inflammatory, analgesic and antithrombotic activity, wherein A is R(COXu)t wherein t is 0 or 1; u is 0 or 1 and X is O, NH, NR1c wherein R1c us a C1-C10 alkyl and R is, for example, (Ia) wherein R1 is acetoxy, preferably in ortho position with respect to -CO- and R2 is hydrogen or acetylsalicylsalicylic acid derivatives; and X1 is the formula (B), Y being a ring containing at least one salified nitrogen atom.
WO2013059582A2 Small molecule inhibitors of histone deacteylases The disclosure relates to small molecules and methods, compositions, and kits comprising these small molecules. In still another embodiment, the disclosure relates to small molecules that inhibit HDAC activity. In yet another embodiment, the disclosure relates to small molecules for inhibiting the growth of cancer cells. In still another embodiment, the disclosure relates to small molecules for reprogramming a cell.
US20120115899 Naphthyridin-2 (1 h)-one compounds useful as antibacterials Compounds of Formula (I), wherein substituents R1, R2 and R5 are as defined, and Ar represents substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, furanyl, imidazolyl and thiophenyl substituted by a hydroxyalkyl substituent and an optional other substituent; compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
CN103211832A Medicine composition containing myricetrin or/and myricetin and application of medicine composition in preparation of medicine used for treating Parkinson The invention relates to a medicine composition of myricetrin or/and myricetin aglycone thereof and levodopa or of levodopa and carbidopa and an application of myricetrin or/and myricetin aglycone thereof as a synergist in preparation of a medicine used for treating Parkinson. In vitro activity determination finds that IC50 of myricetrin and myricetin inhibiting catechol-O-methyltransferase (COMT) can be a micromole-nanomole scale. Rat overall pharmacokinetic study finds that blood concentration of levodopa can be increased after myricetrin and myricetin aglycone thereof and levodopa are used jointly; and myricetrin and myricetin aglycone thereof are high in safety, no obvious toxicity is produced to main visceral organ cells of a human body, and no active intermediate is produced by virtue of metabolism activation and further no damage done to organs such as liver and kidney is initiated, so that the myricetrin and myricetin aglycone thereof have a good application prospect in adjuvant therapy of Parkinson.
US20120134979 Methods and compositions for the treatment of sickle cell disease Presented are mechanism based compositions and methods for treatment of SCD and SCD associated symptoms and disorders, particularly increased RBC sickling, HbS polymerization, hemolysis, tissue congestion and disruption and organ damage or failure in a mammal. The disclosed methods feature the identification of the heretofore unknown role of adenosine levels and signaling in the development of SCD and SCD associated symptoms and disorders. This discovery has lead to the identification of compositions for use as therapies for SCD and SCD associated disorders and symptoms in a mammal.
CN1911220A Injection contg. seven vitamins and taurine An injection for providing vitamins to the patient difficult to eat food is prepared from 7 necessary vitamins including VE, nicotinic acid, pantothenic acid, VB1, VB6, VC and VA, and taurine.
EP1727528A2 Inhibition of mixed lineage kinases and uses therefor Provided herein are methods of using an inhibitor of an MLK protein or polypeptide to inhibit cell proliferation in neoplastic cells, such as for example, a cancer. Such methods may be used to treat a cancer and further may be used in conjunction with administration of an anticancer drug at a reduced dosage to treat a cancer with a concomitant reduction in toxicity to an individual receiving the treatment. Also provided is a method to screen for inhibitory agents to inhibit an activity of a MLK protein or polypeptide and to inhibit cell proliferation of a neoplastic cell having the MLK activity.
US20120252850 Niacin conjugated fatty acid mixtures and their uses The invention relates to niacin conjugated fatty acid mixtures; compositions comprising an effective amount of a niacin conjugated fatty acid mixture; and methods for treating or preventing an metabolic disorder comprising the administration of an effective amount of a niacin conjugated fatty acid mixture.
EP1639991A2 Skin and tissue care and/or treatment composition A composition (I) containing (a) at least one salt selected from alkali metal salts, alkaline earth metal salts and other minerals, additionally contains (b) at least one aminoacid and (c) zinc oxide and/or an inorganic peroxide. - ACTIVITY : Dermatological; antipsoriatic; antirheumatic; cytostatic; gastrointestinal. - MECHANISM OF ACTION : (I) promotes diffusion of ions through ion channels into the intracellular space to improve microcirculation.
CN103040851A Application of Houttuynoid A in preparation of blood sugar reducing medicines The invention discloses an application of Houttuynoid A in preparation of blood sugar reducing medicines. The invention provides a brand-new selection and concept for current anti-diabetic medicines, expands the selective field of anti-diabetic medicines and contributes to development of the technical field. The application of Houttuynoid A provided by the invention is proved to have a remarkable anti-diabetic effect. In the invention, a compound with a explicit chemical structure is selected. The application of Houttuynoid A in preparation of blood sugar reducing medicines is disclosed for the first time. As the framework type belongs to a brand-new framework type and the activity for preventing and treating diabetic is previously unimagined, the probability of giving any inspiration by other compounds is not available, so that the Houttuynoid A has a protruding substantial characteristic and meanwhile is remarkably progressive for treating diabetic.
US20120046256 Lipolytic Methods for Regional Adiposity Comprising Salmeterol or Formoterol Compositions, formulations, methods, and systems for treating regional fat deposits comprise contacting a targeted fat deposit with a composition comprising long acting beta-2 adrenergic receptor agonist and a compound that reduces desensitization of the target tissue to the long acting beta-2 adrenergic receptor agonist, for example, glucocorticosteroids and/or ketotifen. Embodiments of the composition are administered, for example, by injection, and/or transdermally.
WO2008099781A1 Therapeutic or prophylactic agent for demyelinating disease comprising amino alcohol derivative as active ingredient [PROBLEMS] To provide a novel therapeutic or prophylactic agent for demyelinating disease. [MEANS FOR SOLVING PROBLEMS] Disclosed is an amino alcohol derivative represented by the general formula (1) which is a sphingosine-1-phosphate receptor agonist, a pharmacologically acceptable salt of the derivative, or a hydrate of the derivative or the pharmaceutically acceptable salt. The compound can be used as a therapeutic or prophylactic agent for demyelinating disease.
WO2010111464A1 RNA INTERFERENCE MEDIATED INHIBITION OF APOPTOSIS SIGNAL-REGULATING KINASE 1 (ASK1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of ASK1 gene expression and/or activity, and/or modulate a ASK1 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against ASK1 gene expression.
WO2013111729A1 Pharmaceutical composition and quasi-drug cosmetic using same The invention provides a pharmaceutical composition comprising glucose as a tissue repair promoter. The invention further provides a quasi-drug cosmetic comprising the pharmaceutical composition.
EP2385830A1 Treatment of diabetes in patients with inadequate glycemic control despite metformin therapy comprising a dpp-iv inhibitor The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for improving glycemic control in type 2 diabetes patients with inadequate glycemic control despite metformin therapy.
CN102382032A 1-(phenyl)-4-[3-(4-indoxyl)-2-hydroxypropyl]piperazine derivative and salts thereof as well as preparation method and application thereof The invention relates to a structure of an 1-(phenyl)-4-[3-(4-indoxyl)-2-hydroxypropyl]piperazine derivative (the structure is shown as a compound I ) as well as a preparation method and application thereof. The 1-(phenyl)-4-[3-(4-indoxyl)-2-hydroxypropyl]piperazine derivative can be used as a novel retarder for a selectivity alpha1 adrenergic receptor and can be used for relaxing aorta, prostate and bladder neck urethral smooth muscle and treating hypertension, lower urinary tract obstruction or prostatoplasia. The compound and derivatives thereof disclosed by the invention have a simple synthetic path and easiness in operation; and the compound and derivatives thereof have IC50 (muM) to an aortic tissue of chest of a rabbit from New Zealand, which reaches as high as 1.950, and have an excellent action of blocking off the alpha1 adrenergic receptor. In the compound I, R1, R2, R3, R4, R5, R1' and R2' are respectively substituted by hydrogen, alkyl, alkoxy, aryl, substituted aryl, aryloxy, substituted aryloxy and halogen.
EP1194447B1 Novel potassium channels and genes encoding these potassium channels This invention relates to novel potassium channels and genes encoding these channels. More specifically the invention provides isolated polynucleotides encoding the KCNQ5 potassium channel subunit, cells transformed with these polynucleotides, transgenic animals comprising genetic mutations, and the use of the transformed cells and the transgenic animals for the in vitro and in vivo screening of chemical compounds affecting KCNQ5 subunit containing potassium channels.
EP1500656B1 Biguanide derivatives and their use as antidiabetic drugs A therapeutic agent for diabetes which contains as an active ingredient a biguanide derivative represented by the following general formula (1) or a salt thereof: (1) wherein R1, R2, and R3 may be the same or different and each represents one member selected from the group consisting of hydrogen, optionally substituted lower alkyls, and optionally substituted lower alkylthios.
US20100189769 Polypeptide Films and Methods Disclosed herein are polypeptide multilayer films wherein a therapeutic agent is covalently linked to a first layer polypeptide. An advantage of such attachment is that the linked therapeutic agent can be controllably released from the multilayer film into the environment of the film upon the addition of a suitable stimulus. An advantage of the disclosed films and methods is enablement of environmentally-stimulated release under specific conditions.
CN102579699A Composition with function of removing chloasma and preparation method thereof The invention discloses a composition with the function of removing chloasma and a preparation method thereof. The composition is characterized in that the composition takes tribulus terrestris, grape seed extracts and poria cocos as the main functional ingredients; and defined amount of trace elements such as zinc and magnesium can be added; and pharmaceutically acceptable auxiliaries are added to the above ingredients according to a reasonable ratio to prepare various oral preparations, including tablets, capsules, granules, oral liquid and the like. The composition has the functions of relieving mental stress and tranquilizing the mind while playing a role in removing chloasma, is safe and nontoxic and is convenient to use.
US20100029669 3-(substituted ethyl)-rifamycin derivatives useful as antimicrobial agents The present invention is directed to novel 3-(substituted ethyl) rifamycin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.
EP2179661A1 Biscuit comprising guar gum in a rod-like form The present invention relates to a biscuit comprising guar gum characterized in that said guar gum is a native guar gum, in a rod-like form with a length between 0.25 and 8 mm, a width between 0.18 and 2mm and an average length to width ratio between 1.8 and 6. The invention also relates to the use of said biscuit in the diet of subjects suffering from diabetes and especially type 2 diabetes or insulino-resistance to help to control their blood glucose level and a process of manufacturing of said biscuit.
CN101386596A 3-alkylidenehydrazino substituted heteroaryl compounds as thrombopoietin receptor activators 3-alkylidenehydrazino substituted heteroaryl compounds as thrombopoietin receptor activators are provided. A compound is represented by the formula (1), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof, wherein A is a nitrogen atom or CR<4>, B is an oxygen atom, a sulfur atom or NR<9> (provided that when A is a nitrogen atom, B is not NH), R<1> is a C<2-14>; aryl group, L<1> is a bond, CR<10>R<11>, an oxygen atom, a sulfur atom or NR<12>, X is OR<13>, SR<13> or NR<14>NR<15>, R<2> is a hydrogen atom, a formyl group, a C<1-10>; alkyl group or the like, L<2> is a bond or the like, L<3> is a bond, CR<17>R<18>, an oxygen atom, a sulfur atom or NR<19>, L<4> is a bond, CR<20>R<21>, an oxygen atom, a sulfur atom or NR<22>, Y is an oxygen atom, a sulfur atom or NR<23>, and R<3> is a C<2-14>.
WO2014163147A1 Salt of pyrazoloquinoline derivative, and crystal thereof The present invention provides a salt produced from at least one acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, malonic acid, maleic acid, tartaric acid, methanesulfonic acid, benzenesulfonic acid and toluenesulfonic acid and (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1- (tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one or a crystal of the salt, which can be used as an active ingredient for medicines.
CN102114245B Special solvent for daidzein pre-emulsified injection and preparation method and purpose thereof The invention discloses daidzein pre-emulsified concentrated liquid and a preparation and an application of an injection preparation and an enteric-coated preparation thereof. A pharmaceutical composition is mainly prepared by daidzein, an oil-phase emulsifying agent, a latent solvent, a base, an antioxidant and other medicaments according to a conventional method, has significant efficacy for patients with various cardiovascular and cerebrovascular diseases, has the significant characteristics of simpleness in preparation, convenience in use, good stability, fast onset of action and the like, is convenient to store and transport and further has great application prospect.
US20100196500 Anhydrous dicalcium phosphate particles and production method thereof The present invention provides anhydrous dicalcium phosphate particles which satisfies the conflicting requirements of the improvement of handling properties such as high flowability and a small bulk and the improvement of tableting properties at the same time during preparation and a method of producing the same. The method of producing anhydrous dicalcium phosphate by heating water suspensions of a phosphoric acid compound and a calcium compound at 50 to 100° C., comprises the step of: heating the phosphoric acid compound and the calcium compound at 75° C. or higher in advance to carry out a neutralization reaction in the presence of an alkali to obtain agglomerated anhydrous dicalcium phosphate particles.
CN103479593A Preparation method for omeprazole enteric coated tablet The invention relates to a preparation method for an omeprazole enteric coated tablet. The components comprise in percents by weight: 10-50% of omeprazole, 1.25-6.25% of superfine silica powder, 30-78% of lactose, 2-3% of copolyvinylpyrrolidone, 5-12% of crospovidone, 1.5-2.0% of sodium octadecyl fumarate and 0.5-1.0% of magnesium stearate. The preparation method comprises: uniformly mixing micronized omeprazole and superfine silica powder, sieving; sieving copolyvinylpyrrolidone, crospovidone, lactose and sodium octadecyl fumarate, uniformly mixing with omeprazole and superfine silica powder, adding into a drying-method granulator, granulating for 3-4 times, screening out integrated particles with a 60 mesh sieve and obtaining dry particles; blending uniformly the dry particles and magnesium stearate by a three-dimensional mixer, adding into a tablet press for pressing tablets; and then coating to obtain the omeprazole enteric coated tablet. The formula is simple; the preparation method helps to solve the industrialized production problem of omeprazole enteric coated tablet high-specification products such as a product with a specification of 40 mg/tablet; and the preparation is controllable in quality, the product is good in uniformity, and impurity content is low.
US20100266527 Anti-microbial polymers and their compositions Polymers derived directly from acrolein monomer that are substantially soluble in water and/or aqueous media, together with methods for preparing same and compositions containing such for use as an anti-microbial, anti-cancer, anti-inflammatory and/or anti-coagulant.
US8247448 Butenoic acid derivatives, processes for the preparation thereof, pharmaceutical compositions comprising them, and use for the treatment of dyslipidaemia, atherosclerosis and diabetes The present invention relates to butenoic acid derivatives of the formula I: in which R, R1, R2 and R3 are as defined in the description, and also to processes for the preparation thereof, to pharmaceutical compositions comprising them and to their use for the treatment of dyslipidaemia, atherosclerosis and diabetes.
US20090082362 Use of capsaicin receptor antagonists to treat symptoms of tear gas exposure Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.
EP1395583B1 New phenylpiperazines The invention relates to novel phenylpiperazine derivatives of the formulawherein:- R represents the group (a) or (b) as indicated in the description. These compounds are (partial) D2 receptor agonists and are usefull for treating CNS disorders, in particular Parkinson's disease.
EP2085398A1 Pyrazolopyrimidines, a process for their preparation and their use as medicine The invention relates to pyrazolopyrimidine derivatives of Formula I wherein R1 represents chloro or bromo; A represents as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.
US20080261994 4-[5-((1S,2R)-1-Carboxy-2-phenyl-cyclopropylsulfamoyl)-thiophen-2-yl]-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester; aggrecanase and matrix metalloproteinase (with zinc in the catalytic active center) inhibitor; antiarthritic agent: osteoarthritis, rheumatoid arthritis The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
WO2010024956A3 Antihistamine and antihistamine-like nasal application, products, and method A method of and product for reducing the undesirable effects of allergic rhinitis by applying a formulation to a person's nasal region or nostrils. The formulation creates a barrier that prevents airborne allergens from contacting nasal mucous membranes, and at the same time, electrostatically repels or attracts and captures the particulate allergens, and changes their shapes so as to mitigate the effects of allergic rhinitis. The formulation may be made more effective by the addition of an anti-histamine compound.
US20090069295 Deuterium-enriched conivaptan The present application describes deuterium-enriched conivaptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
EP1697397A1 Cobalamine derivatives useful for diagnosis and treatment of abnormal cellular proliferation The invention relates to cobalamin derivatives (a) having no binding affinity or low binding affinity to the transport protein transcobalamin II TCII) and (b) retaining activity as a vitamin B12 substitute, optionally carrying a therapeutic and/or diagnostic agent, such as a radioactive metal. These compounds have a much reduced accumulation rate in blood and benign organs, such as kidney and liver, compared to the accumulation rate in neoplastic tissues, and are more rapidly eliminated from blood. The invention further relates to a method of diagnosis and a method of treatment of a neoplastic disease or an infection by microorganisms in a mammal comprising (a) exposing the mammal to a period of a vitamin B12 - free diet, and (b) subsequently applying a cobalamin derivative of the invention carrying a diagnostic and/or therapeutic agent. By selecting cobalamin derivatives acting as vitamin B12 substitutes, the risk of the formation of resistant offspring in neoplastic tissue is much reduced.
US20110020232 Cancer treatment with gama-secretase inhibitors Provided are methods for treating cancer in a patient, comprising administering to a patient in need thereof a therapeutically effective regimen, the regimen comprising administering a gamma-secretase inhibitor, wherein the regimen results in a reduction in the cancer cell population in the patient. In some embodiments of the methods, the therapeutically effective regimen stabilizes, reduces or eliminates the cancer stem cell population. Also provided are compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, and X are as herein described.
CN102166357A Medicinal composition containing bicyclic aza-alkane derivative The invention relates to a medicinal composition which comprises a bicyclic aza-alkane derivative as shown in formula (I), at least one medicine for treating cardiovascular and cerebrovascular diseases and a pharmaceutically acceptable carrier. The invention also relates to a medicine box containing the medicinal composition. The medicinal composition or the medicine box is used for preventing, alleviating or treating the following diseases or symptoms: type II diabetes, diabetic complications, hyperglycemia, obesity, insulin resistance, hypertension, hypertension complications, dyslipidemia, coronary heart diseases, angina, congestive heart failure, arrhythmia, cerebral apoplexy, arteriosclerosis, cerebral infarction, ischemic diseases, cerebrovascular diseases, cardiovascular diseases, coronary artery diseases, sexual dysfunction, cognitive dysfunction, ventricular dysfunction, cardiac insufficiency, pulmonary vascular diseases or renal vascular diseases. The medicinal composition reduces the incidence and/or death rate of cardiovascular and cerebrovascular diseases, reduces adverse reaction, and improves the compliance of patients for taking.
CN101961369A Formula of medicament for treating cervical spondylosis The invention relates to a formula of an externally applied medicament for treating cervical spondylosis and arthralgia. The technical scheme is that the medicament consists of the following components in part by weight: 100 to 200 parts of safflower, 10 to 80 parts of borneol, 10 to 80 parts of pseudo-ginseng, 1 to 8 parts of musk and 50 to 150 parts of cedar. The medicament of the invention has the effects of diminishing inflammation, relieving pain and activating blood circulation to dissipate blood stasis; and when used, the medicament is crushed and packaged into cloth bags and placed at a cervical vertebra part together with a heat source.
EP0861236B2 Cyclic and heterocyclic n-substituted alpha-iminohydroxamic and carboxylic acids Compounds of formula (I) are suitable for use in the production of medicaments used for treating disorders associated with increased activity of matrix-degrading metalloproteinases.
CN101554373B Caffeic acid composition and preparation method thereof The invention relates to a caffeic acid composition which is characterized by comprising an A composition, a B composition, surface active agent, quick-effect disintegrant and lubricant; the A composition is caffeic acid and a medicinal accessory, and the B composition is a medicinal accessory; the weight ratio of the A composition and the B composition ranges from 1: 5.5 to 1: 1; and the caffeic acid accounts for 10-50 percent (W \ W) of the A composition. The standard of the caffeic acid composition is 0.95-0.105 weight part, wherein 0.1 weight part is the best. The caffeic acid composition and the preparation method thereof solves the problems concerning fast medicine disintegration and fast medicine effect and in particular greatly improves the bioavailability and the tablet stability of a caffeic acid tablet in the body.
WO2005072292A3 Methods for enhancing radiation therapy Methods of treating cancer are provided. The methods are improved methods of radiation therapy involving administering an IGF-1-receptor agonist along with therapeutic radiation to a mammal afflicted with cancer. The IGF-1-receptor agonist causes the cancer cells to divide and move into more sensitive stages of the cell cycle, sensitizing the cancer cells to be killed more efficiently by radiation. Also provided are methods of treating cancer involving administering radiation to a mammal together with administering a growth-hormone agonist, an insulin-receptor agonist, or sugar.
US20100152268 Stable atorvastatin formulations The present invention provides novel alternative pharmaceutical compositions comprising amorphous atorvastatin or a pharmaceutically acceptable salt thereof and a controlled amount of one or more additional compounds selected from the group consisting of compounds of formula I (formed by ring opening of the epoxide of Formula II to form a diketo dihydroxy derivative), II (diketo epoxide derivative), III (di-epoxide derivative formed by ring closure of the heptanoic acid chain to form a cyclohexanoate substituent), IV (2-oxo derivative with the isopropyl group rearranged to the 3-position) and V (phenantrene derivative of the 2-oxo derivative), together with one or more suitable pharmaceutical excipients, which compositions have improved stability.
WO2009137201A1 Triazolopyridinone derivatives for use as stearoyl coa desaturase inhibitors The present invention discloses triazolopyridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.
WO2010054452A1 New compounds of the pterocarpanquinone family, method for preparing the same, pharmaceutical composition containing the new compounds of the pterocarpanquinone family, uses and therapeutic method The invention belongs to the chemical pharmaceutical field, and the new compounds of the pterocarpanquinone family having formula (I) according to the invention can be reduction activated, generating alkylating species in the intracellular medium, and exhibit a selective cytotoxic effect, in particular for constantly dividing animal cells of human and/or non-human mammals; they are therefore useful for the treatment of diseases and/or disorders related to the phenomenon of undesirable cell proliferation. These compounds are also effective for the treatment of diseases and/or disorders related to a rise in THF-α in human and non-human mammals and to the method for producing these compounds, to pharmaceutical compositions containing said compounds of formula (I), to the use of said compounds of formula (I), to a medicament containing said compounds and to treatment methods.
US7977485 2-heteroaryl carboxamides The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
WO2007049818A1 Anti-fatty liver, anti-obesity or hypolipidemic composition Disclosed are: an anti-fatty liver or anti-steatohepatitis composition comprising lysine in an amount of not less than 5.0% and less than 65.0%, threonine in an amount of not less than 5.0% and less than 65.0%, leucine in an amount of not less than 1.0% and less than 35.0%, isoleucine in an amount of not less than 1.0% and less than 35.0% and valine in an amount of not less than 1.0% and less than 35.0% by mole relative to the total amount of the amino acids contained in the composition; and an anti-obesity or hypolipidemic composition which comprises lysine, threonine, leucine, isoleucine and valine in the same amounts as those mentioned above and does not contain at least one non-essential amino acid selected from the group consisting of proline, glycine, tyrosine and arginine.
CN102210783B Composition preparation of donkey-hide glue, and preparation method thereof The invention discloses a composition preparation of donkey-hide glue, and a preparation method thereof, in particular a donkey-hide glue soft capsule and a preparation method thereof. The donkey-hide glue soft capsule is composed of the following components in parts by weight: 40-65 parts of donkey-hide glue, 6-14 parts of vitamin C, 2-8 parts of heme, 20-35 parts of red jujube, 10-25 parts of camellia oil, 5-12 parts of dangshen, 0.1-0.5 part of sucrose fatty acid ester and 7-15 parts of water. The donkey-hide glue soft capsule is capable of nourishing yin and moisturizing the lung, invigorating qi and tonifying the blood, achieves the effects on supplementing iron and tonifying the blood simultaneously, and especially has better effect on tonifying the blood for iron-deficiency anemia.
US20050176685 Administering bisphosphonate compounds such as ibandronate, minodronate, pamidronate, risedronate, zoledronate, and alendronate; osteoporosis Composition and method for preventing or treating abnormal bone resorption in mammals, the composition characterized as containing, a supplementary effective amount of a non-activated metabolite of vitamin D2 and/or D3 and a pharmaceutically effective amount of bisphosphonate to provide vitamin D nutrition during treatment to facilitate normal bone formation and mineralization, while minimizing the occurrence of or potential for the complications associated with vitamin D insufficiency, such as hypocalcemia and osteomalacia. The method of preventing or treating may be further characterized by concomitantly administering the components simultaneously or alternately at dosing intervals selected from once-weekly, twice-weekly, bi-weekly, monthly, and bimonthly.
EP2178540A1 Pharmaceutical composition suitable for adsorption to the cell surface of pathogenic microbes The present invention provides a pharmaceutical composition comprising a product for adsorption purposes, preferably in particulate or polymeric form, consisting of an in water insoluble or swelling support matrix wherein the support matrix is substituted with a hydrophobic entity which in turn is connected to a positively charged entity, other than said in water swelling or insoluble support matrix, and/or a product for adsorption purposes comprising a first support matrix connected to a hydrophobic entity and a second support matrix connected to a positively charged entity, and/or a product for adsorption purposes consisting of an in water insoluble or swelling support matrix wherein the support matrix is substituted with a hydrophobic entity and a positively charged entity, and/or a product for adsorption purposes consisting of an in water insoluble or swelling support matrix wherein the support matrix is substituted with a hydrophobic entity, and/or one or more preservatives, and/or one or more artificial antibodies and optionally a carrier. Also medical use of said product, use of said product for the manufacturing of a medicament for treating pathogenic microbes and therapeutic use of said product is provided.
CN101899047A Beta-amino tetrahydropyrazine, tetrahydropyrimidine and tetrahydropyridine used as dipeptidy peptidase inhibitors for curing or preventing diabetes The invention relates to beta-amino tetrahydropyrazine, tetrahydropyrimidine and tetrahydropyridine used as dipeptidy peptidase inhibitors for curing or preventing diabetes. Each variable quantity is defined as the application specification. The compounds are the inhibitors of dipeptidy peptidase-IV enzyme ('DP-IV inhibitors') and can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete. The invention also relates to a medicinal composition comprising the compounds and application of the compounds and the composition in preventing or curing the diseases relevant to the dipeptidy peptidase-IV enzyme.
US20070053982 Sustained release oral formulations Pharmaceutical composition capable of releasing a therapeutically effective dose of active agent, e.g., rivastigamine, in a time-controlled manner.
WO2009052226A1 Crystalline indazole-derived chemotherepeutic N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N'-(2-fluoro-5-methylphenyl)urea Hydrate Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed.
WO2006050544A3 Tolperison for treating dogs having degenerative spinal symptoms The invention relates to a veterinary medicinal preparation for oral administration for treating mammals such as dogs having degenerative spinal symptoms. This preparation contains, as an active ingredient, tolpersion together with at least one additive commonly used in veterinary medicine. A series of clinical signs in postoperative form or also during the preparation of possible surgical operations or during a long ongoing treatment carried out without possible surgical operations can be treated insofar as tolpersion is used as racemate in the form of its isomer mixture, in which the R(-) isomer is enriched in this mixture.
CN102260291B Riboflavin sodium phosphate crystalline compound and preparation method thereof The invention relates to a riboflavin sodium phosphate crystalline compound, which comprises 1.5 crystal waters. The riboflavin sodium phosphate crystalline compound is measure by using Cu-Kalpha rays. Characteristic peaks are shown when X-ray powder is diffracted at 2theta of 6.1 DEG, 11.2 DEG, 13.4 DEG, 14.8 DEG, 19.7 DEG, 20.8 DEG, 23.9 DEG, 24.5 DEG, 26.9 DEG, 27.7 DEG, 29.1 DEG, 31.0 DEG, and 31.6 DEG. The invention also relates to a preparation method of the compound, and a pharmaceutical composition containing the compound. The invention further relates to a synthesizing method of riboflavin sodium phosphate. As a result of experiments, the riboflavin sodium phosphate crystalline compound provided by the invention has high stability.
US20080146567 5-HT5A receptor antagonists; depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, drug withdrawal The present invention relates to 2-Aminoquinoline derivatives of general formula I and pharmaceutically-acceptable acid-addition salts thereof, wherein R1, R2 and X are as defined in the specification. The compounds may be used as 5-HT5A receptor antagonists. The present invention relates also to processes for making such a compound and a pharmaceutical composition comprising such a compound. Compounds of the present invention are useful in the prevention and/or treatment of anxiety depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders and gastrointestinal disorders.
CN101708153A High dispersion preparation containing riboflavin derivative The invention discloses a high dispersion preparation containing a riboflavin derivative, selected from a lipidosome, nonionic surfactant vesicles, particles, nano-particles, a nano-suspension, an emulsion and micelle. The riboflavin derivative can be used as a prodrug for preventing and treating riboflavin deficiency of human bodies, and the high dispersion preparation containing the riboflavin derivative has the functions of preparation stability improvement, absorption promotion, bioavailability enhancement, targeting, slow release, controlled release, patient compliance enhancement and the like.
WO2014106606A1 Nove phenyl/pyridine series substitued by hydroxyethylamino for the treatment of cancer The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and W are as described herein, compositions including the compounds and methods of using the compounds.
WO2006023395A3 4-(2,4-dichloro-5-methoxyphenyl)amino-6-methoxy-7-{[5-(substituted-amino)methyl]-3-furyl}-3-quinolinecarbonitriles as kinase inhibitors This invention relates to compounds having the structure of Formula (I) wherein R1, R2, R3, and R4 are described herein.
CN103721267A Composition containing desloratadine citrate disodium The invention relates to a composition containing desloratadine citrate disodium. The composition adopts the dosage form of granules; the combination of cyclodextrin and desloratadine citrate disodium in a specific proportion is adopted; the cyclodextrin is used for wrapping the desloratadine citrate disodium, so as to decrease the degradation of the desloratadine citrate disodium in active auxiliary materials such as monose, and biose, and the stability of the desloratadine citrate disodium is effectively enhanced. Accelerated tests and long term tests prove that the stability of the medicine during the storage process can be soundly ensured, in addition, due to the addition of a proper corrigent, the taste of the medicine is improved. Therefore, the composition is particularly suitable for children or patients suffering from dysphagia.
CN101757511A Medicine composition for treating acute and chronic neutrophilic leukemia and preparation method thereof The invention discloses a medicine composition for treating acute and chronic neutrophilic leukemia, which is prepared from the following raw medicinal herbs: 10-50 parts of dehydrated dulcite, 30-50 parts of red flower, 30-50 parts of astragalus mongholicus, 15-50 parts of rhizoma sparganii, 15-50 parts of root of red-rooted salvia, 15-50 parts of trogopterus dung and 10-30 parts of radix scrophulariae. The invention has remarkable treatment effect on leukemia, a certain treatment effect on lung cancer, myeloma multiplex, nasopharyngeal darcinoma and the like, better recent treatment effect especially on the acute and chronic neutrophilic leukemia with remission rate of 86 percent, higher effective rate of various lung cancers and lower toxic and side effects.
WO2012012798A2 Materials and methods for reduction of protein tau and treatment of neurodegenerative diseases The subject invention provides a myricanol compound that is in predominant form of (+)-αR,11S-myricanol as compared to (-)-αS,11R-myricanol. In one embodiment, the (+)- αR,11S-myricanol is isolated from Myrica cerifera, and is in about 86% enantiomeric excess of (-)-αS,11R-myricanol. The subject invention also pertains to therapeutic compositions and methods for treatment of neurodegenerative diseases, in particular, neurodegenerative diseases associated with abnormal accumulation of protein tau. Specifically exemplified herein is the therapeutic use of myricanol and myricanone isolated from root barks of Myrica species. Also provided are methods for preparing extracts of the subject invention from Myrica species.
WO2012119010A3 Materials for inhibiting aromatase and method of using the same to diagnose, treat and monitor breast cancer Disclosed herein are triphenylalkenes that can be used to inhibit aromatases. The inhibitory potency order of the tested compounds was as follows: norendoxifen » 4,4'-dihydroxy- tamoxifen > endoxifen > N-desmethyl-tamoxifen, N-desmethyl-4'-hydroxy-tamoxifen, tamoxifen-N-oxide, 4'-hydroxy-tamoxifen, N-desmethyl-droloxifene > 4-hydroxy-tamoxifen, tamoxifen. Norendoxifen inhibited recombinant aromatase via a competitive mechanism with a K i of 35 nM. Norendoxifen inhibited placental aromatase with an IC50 of 90 nM, while it inhibited human liver CYP2C9 and CYP3A with IC50 values of 990 and 908 nM respectively. Inhibition of human liver CYP2C19 by norendoxifen appeared even weaker. No substantial inhibition of CYP2B6 and CYP2D6 by norendoxifen was observed. These compounds, and pharmaceutically acceptable formulations of these compounds, can be used to treat diseases, diagnose and monitory conditions, including some forms of breast cancer. Such compounds can be used alone or in combination with other therapies and therapeutic compounds for treating diseases such as cancer.
US8124592 Development of a preventive vaccine for filovirus infection in primates The present invention relates generally to viral vaccines and, more specifically, to filovirus vaccines and methods of eliciting an immune response against a filovirus or disease caused by infection with filovirus.
CN101062394A Method for detecting the quality of pill for strengthening spleen and intestines The invention discloses a quality detection method for intestine-tonifying pills, which comprises carrying out gradient elution through high performance liquid phase chromatographic method, measuring the content of peony glycosides, meladinin and isopsoralen simultaneously, thereby achieving accurate certification for the available compositions under optimum mobile phase and maximum absorption wave length condition.
WO2009044141A1 Compositions comprising cetirizine and a non beta-2-adrenoreceptor agonist, a beta-2-adrenoreceptor agonist or an anti -inflammatory and the use thereof for the treatment of respiratory disorders There is described a pharmaceutical composition comprising a therapeutically effective amount of cetirizine, or a pharmaceutically acceptable derivative thereof, and a therapeutically effective amount of one or more compounds selected from the group consisting of a non beta-2-adrenoreceptor agonist; a beta-2-adrenoreceptor agonist and an anti-inflammatory agent; in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier.
US20090075945 Phosphate-bearing prodrugs of sulfonyl hydrazines as hypoxia-selective antineoplastic agents Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Methods of treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. where R is C1-C10 alkyl or haloalkyl; R′ and R″ are each independently C1-C10 alkyl; and R1 is C1-C10 alkyl, or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.
US7109234 Benzoxathiepine derivatives and their use as medicines The invention concerns 3-arylthio-propyl-amino-3,4-dihydro-2H-1,5-aryloxathiepin derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a hydrogen atom, a fluorine atom or a chlorine atom, a hydroxy group, an alkyl, cyclopropyl, alkoxy, cyclopropoxy radical or when they occupy adjacent positions, form with the carbon atoms bearing them a carbon-containing cycle or an oxygen-containing heterocycle with five non-aromatic rings; R3 represents an alkyl radical, a hydroxy group or a methoxy radical; R4 represents a hydrogen atom or a methyl radical; and R5 and R6, identical or different represent a hydrogen atom, an alkyl, alkoxy, alkylthio, alkylamino radical, or the groups OR4 and R5 form with the carbons which bear them a non-aromatic heterocycle with five or six rings containing at least an oxygen atom; and their pharmaceutically acceptable additions salts
US20120083515 Bioadhesive gel based on hydroxyethylcellulose Disclosed are compositions in the form of a bioadhesive gel that adheres to the mucous membranes, in particular the vaginal mucosa, for the application of active ingredients and/or principles, comprising hydroxyethylcellulose as the only gelling agent.
CN101249179A Medicine for external application for curing hyperosteogeny and disc herniation and method of preparing the same The invention discloses an external medicine for treating hyperosteogeny and disc herniation and a preparation method. The external medicine has the raw ingredients and weight parts that: pangolin is 10 to 20, agkistrodon acutus is 10 to 20, saffron is 5 to 15, panax notoginseng is 10 to 20, radix cyathulae is 5 to 15, kudzu roots are 15 to 30, herba lycopodti is 10 to 20, olibanum is 10 to 15, dog bones are 20 to 30, eucommia bark is 10 to 20, wild celery is 5 to 10, and musk is 0.2 to 0.5. The invention has the preparation method that: the raw ingredient medicines are mixed and crushed into powders which are mixed into a paste by adding with rice vinegar; after the paste is evaporated for 15 to 20 minutes under water insulation, the rice vinegar is bedashed in; the evaporation is continued for 5 to 10 minutes; or the raw ingredients are crushed into powders which are mixed evenly and stir-fried until done, and then the powders is made into a plaster for bonding application through mixing with vinegar or water. The external medicine and the preparation method have the advantages of good curative effect, short course of treatment, hard relapse, no toxic side effects, and low treatment cost by apply the external medicine to act the external application on patients.
CA2533649A1 Combined treatments comprising synthetic peptide copolymers for preventing graft rejection The present invention provides compositions and methods for the treatment of graft rejection associated with transplantation of tissues and organs. More specifically, the compositions and methods of the present invention relate to combined treatment involving at least one agent selected from Copolymer 1, a copolymer 1-related heteropolymer or an ordered peptide in combination with at least one additional known immunosuppressive agent. The present invention also provides compositions and methods for the treatment of graft rejection using ordered peptides or ordered copolymer 1-related heteropolymers as monotherapy.
US20080076757 Medicine for treating gastrointestinal disorder including irritable bowel syndrome A method of treating a spinal injury in a patient presenting symptoms comprising irritable bowel syndrome, the method including administering a dose of a medicine to the patient presenting the irritable bowel syndrome, the medicine including a tricyclic antidepressant and a stool softener, in which the dose contains a quantity of the tricyclic antidepressant determined to be effective to treat the irritable bowel syndrome in combination with the stool softener but to be not effective to treat any psychiatric disorder in the patient.
WO2007037518A1 Mutilin derivative and pharmaceutical composition containing the same The invention is intended to provide a novel compound which is useful as an antibacterial agent and a manufacturing intermediate thereof and relates to a mutilin derivative represented by the formula (I) which is useful as an antibacterial agent against a multidrug resistant organism, a manufacturing intermediate thereof and the like. In the formula (I), R1 represents an ethyl group or a vinyl group, P1 represent H or a protecting group for a hydroxy group, R2 and R3 represent H or the like, G represents CH2 or the like, A represents -S-, -SO2-, -O- or the like, m represents an integer of 0 to 4, the Q1 ring represents a saturated heterocyclic group, R4 represents H, a lower alkyl group or the like, and W represents a group represented by the formula (W-1) or an amino protection group. In the formula (W-1), X represents a lower alkylene chain, a single bond or the like, Z1 represents CH or the like, Z2, Z3 and Z4 represent N or the like, and Y1 and Y2 represent H, an amino group, a group represented by the formula (Y-1) or the like. In the formula (Y-1), the Q2 ring represents a saturated heterocyclic group, and R9 and R10 represents H, a lower alkyl group or the like. (I) (W-1) (Y-1)
US20090298752 Aplidine treatment of cancers Aplidine demonstrates considerable promise in phase (I) clinical trials for treatment of tumors, and various dosing regimes are given. Tumor reduction has been observed in several tumor types including renal carcinoma, colorectal cancer, lung carcinoid, medullary thyroid carcinomas and melanoma. It has also been found that aplidine has a role in inhibiting angiogenesis, complementing the anti-tumor activity.
CN101578098A Drug, drug induction device, magnetic detector and method of designing drug It is intended to provide a drug delivery system which makes it possible to solve the existing technical problems and is easily usable in practice. A drug, which comprises an organic compound or an inorganic compound and has been magnetized by modifying a side chain and/or crosslinking side chains, is induced by a magnetic force into target tissues or an affected part.
US20120149766 Dietary and pharmaceutical compositions comprising a sage extract containing a mixture of tricyclic diterpenes and their derivatives and their uses The present invention refers to a sage extract containing a mixture of tricyclic diterpene (derivative)s of the formulae I to III, preferably to a sage extract containing a mixture of tricyclic diterpene (derivative)s of the formulae I to IV, more preferably to a sage extract containing a mixture of tricyclic diterpene (derivative)s of the formulae I to V, for use as medicaments for the treatment of a disorder connected to reduced neurotransmission, as well as to dietary and pharmaceutical compositions and their uses.
US7176228 Amidobiphenyloxime derivatives, useful as fungicide or bactericide for protection of crops and materials The invention relates to biphenylcarboxamides of the formula (I) in which A, R, Z, X, Y, m and n are each as defined in the disclosure, to a plurality of processes for preparing these substances, to their use for controlling undesirable microorganisms, and to novel intermediates and their preparation.
CA2595573A1 Methods of treating mesothelioma using an antisense oligonucleotide to thymidylate synthase Provided are methods for the treatment of mesothelioma in an animal, comprising the use of an antisense oligonucleotide complementary to a sequence from thymidylate synthase, and the use of the combination of the antisense oligonucleotide complementary to a sequence from thymidylate synthase and a chemotherapeutic agent.
US20050124592 Administering tibolone to female patients to treat estrogen-deficiency related, climacteric complaints exhibited while the female patients are being treated with a drug to prevent the biosynthesis of endogenous estrogen; aromatase inhibitors to prevent bone loss; reduced side efffcts for cancer patients Disclosed is a treatment of estrogen-deficiency related complaints in females that exhibit these complaints while they are on treatment with a drug which prevents the synthesis of endogenous estrogen. Such drugs are, e.g., anti-cancer drugs such as aromatase inhibitors. The invention resides in the use of tibolone, which has an unexpectedly beneficial working in this particular patient group in that it does not stimulate breast, while preventing bone loss and relieving climacteric complaints in a patient group in which this is more difficult than in any other group due to the nature of the concomitant cancer treatment (no circulating estrogen making for a higher severity of the complaints, the lack of effect on the estrogen receptor making for an increased risk associated with estrogenic breast stimulation once estrogen-like compounds are administered.
CN101544578A Preparing method for phenyl acetic acid derivates and applications in medicament The invention discloses phenyl acetic acid derivates shown in general formula (I), a preparing method and applications in medicament. The compound has the insulin sensitization activity, thus it can be used for preparing the antidiabetic medicament and decreasing blood sugar concentration of the diabetes patient and preventing the complication generation of the diabetes patient.
CN101701008A Compound separated and extracted from lotus leaf The invention discloses a 2-hydroxy-1-methoxyl-6-methyl-6a, 7-dehydro aporphine compound, an extracting and separating method thereof, and a structure identifying method. The chemical structure of the 2-hydroxy-1-methoxyl-6-methyl-6a, 7-dehydro aporphine compound of the invention is as follows. The 2-hydroxy-1-methoxyl-6-methyl-6a, 7-dehydro aporphine compound of the invention having analgesic activity is proved by experiment.
WO2014068070A1 Methods for preventing antiphospholipid syndrome (aps) The present invention relates to the prevention or treatment of antiphospholipid syndrome (APS) in a patient in need thereof (e.g. patients affected with primary APS, a secondary APS, a catastrophic APS (CAPS) or a transplant recipient with antiphospholipid antibodies (APA)). The present invention also relates to the prevention APS-related vascular lesions in said a patient in need thereof. The present invention further relates to PI3K–AKT–mTOR pathway inhibitor for use in inhibiting endothelial m TORC activation triggered by APA in a patient in need thereof.
CN102895178A Strong solution-type moxifloxacin hydrochloride injection and preparation method thereof The invention relates to a strong solution-type moxifloxacin hydrochloride injection containing a non-sulfur-containing amino acid or a pharmaceutically acceptable salt thereof, and preparation method thereof. The solvent used in the strong solution-type moxifloxacin hydrochloride injection is smaller in dosage, with better security, and simultaneously has a more significant effect for improving solubility and stability of the moxifloxacin hydrochloride strong solution; the quality of prepared injections is more stable; and preparation process is simple, and easy to operate.
CN103739657A Camellia saponin compound, preparation method, and application thereof, and anti-tumor drug prepared by using camellia saponin compound The invention belongs to the technical field of medicinal chemistry, and discloses a camellia saponin compound, a preparation method, and application thereof, and anti-tumor drug prepared by using camellia saponin compound. The camellia saponin compound has a structure shown in formula I. The camellia saponin compound which has a certain inhibiting effect on hepatoma carcinoma cells, breast cancer cells, melanoma cells and lung cancer cells and can effectively inhibit the growth of liver tumors, so that the camellia saponin compound has obvious anti-tumor activity and can be applied for preparing the anti-tumor drugs. (The formula I representing the structure of the camellia saponin compound is shown in the specification.).
US20070287693 Benzamide Derivatives That Act Upon The Glucokinase Enzyme Compounds of Formula (I): wherein R1 is hydroxymethyl; R2 is selected from —C(O)NR4R5, SO2NR4R5, S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted hererocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from, for example, hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is, for example, an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
WO2012173634A1 Systems and methods for balancing and maintaining the health of the human autonomic nervous system A protocol or procedure is provided for lowering sympathetic nervous system arousal in a person in order to prepare that person for a medical or dental procedure. First, a therapeutic dosage of one or more neurotransmitter supplements, such as a gamma aminobutyric acid formulation, a tryptophan-derived neurotransmitter precursor, and dehydroepiandrosterone are administered to the patient. Concomitantly, gelled electrodes are placed adjacent or below the mastoid. The gelled electrodes are connected to a cranial electrotherapy stimulation device that administers a sub-sensation level current to the patient. Also, a noise dampening headset is placed on the patient and a neuroacoustic entrainment recording or program is played. Next, light is blocked with black out glasses. Then, the medical or dental procedure is performed.
US7135196 Iron compositions Compositions in solid form, such as powders, comprising a mixture of a ferrous salt and a hydroxypyrone maybe used to increase the level of iron in a patient's bloodstream or to treat and/or prevent gastrointestinal infection.
US7435742 potent antagonists of M3 muscarinic receptors; chronic obstructive pulmonary disease; bronchitis, bronchial hyperreactivity, asthma, cough and rhinitis; gastrointestinal disorders; incontinenc; [2-(3,4-Dimethoxyphenyl)ethyl]-(5-methylfuran-2-ylmethyl)carbamic acid (3R)-1 -azabicyclo[2.2.2]oct-3-yl ester Carbamates of formula (I) or pharmaceutically acceptable salts thereof, including quaternary ammonium salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.
WO2009053654A2 Gemcitabine phosphoester prodrugs as anticancer agents The present invention relates to gemcitabine phosphoester prodrugs with antitumour activity, of formula (I) in which n, Y, Z and Ri are as defined in claim 1, and also the pharmaceutical compositions comprising such a compound, in combination with at least one pharmaceutically acceptable excipient, and the use of such a compound for preparing an antitumour or anticancer medicament.
WO2008007107A1 Tetrahydrofuro (3, 2-b) pyrrol-3-one derivatives as inhibitors of cysteine proteinases Compounds of formula (I) and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget' s disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain. Compounds (I) are cysteine protease inhibitors.
CN102008466A Febuxostat medicament composition and preparation method thereof The invention relates to a febuxostat medicament composition and a preparation method thereof. The febuxostat medicament composition is characterized in that: the flavoring agent in the febuxostat medicament composition is selected from gelatin, mannitol or aspartame; the medicament composition exists in a form of powder or granules; and the preparation has good stability, covers the bitter taste, has good mouthfeel, quick disintegration and quick absorption, and is convenient to carry.
US20090087416 novel B7-H3 and B7-H4 polypeptides useful for co-stimulating T cells, vectors containing the nucleic acid molecules, and cells containing the vectors The invention provides novel B7-H3 and B7-H4 polypeptides useful for co-stimulating T cells, isolated nucleic acid molecules encoding them, vectors containing the nucleic acid molecules, and cells containing the vectors. Also included are methods of making and using these co-stimulatory polypeptides.
US20120077769 Topical ophthalmic compositions containing tobramycin and dexamethasone Ophthalmic pharmaceutical compositions containing tobramycin, dexamethasone and deacetylated xanthan gum are described. The compositions provide longer ocular retention for enhanced ocular bioavailability of tobramycin and dexamethasone. In a preferred embodiment, the compositions also provide for improved suspension of dexamethasone. The concentration of ionizable species in the compositions is controlled so as to prevent precipitation of the xanthan gum as a result of ionic interactions between tobramycin and xanthan gum, while allowing for a restoration of viscosity upon topical application of the compositions to the eye. The use of deacetylated xanthan gum is disclosed, so as to avoid formulation instability caused by pH drift during storage.
US8343942 Methods for treating interstitial cystitis Described herein are methods for treating interstitial cystitis in a subject comprising administering to the subject an effective amount of a compound which is a modified hyaluronan or a pharmaceutically acceptable salt or ester thereof, wherein said hyaluronan or its pharmaceutically acceptable salt or ester comprises at least one sulfate group and the primary C-6 hydroxyl proton of at least one N-acetyl-glucosamine residue is substituted with an unsubstituted alkyl group or fluoroalkyl group.
CA2630818A1 Pharmaceutical composition for prevention or treatment of neurogenic pain Disclosed is a pharmaceutical useful for the prevention or treatment of a neurogenic pain. Specifically, disclosed is a prophylactic or therapeutic agent for a neurogenic pain (e.g., painful diabetic neuropathy, post-herpetic neuralgia, trigeminal neuralgia or chronic post-operative or post-traumatic pain), which comprises a .beta.3-adrenergic receptor stimulator as an active ingredient. Also disclosed is a combination pharmaceutical comprising a combination of a .beta.3-adrenergic receptor stimulator and at least one substance selected from the group consisting of a neurotropic vitamin preparation, a nonsteroidal antiinflammatory agent, an aldose reductase inhibitor, a lidocaine-like antiarrhythmic agent, an antidepressant agent and an anticonvulsant agent.
US20120232100 Solid forms of 3-(5-amino-2-methyl-4-oxo-4h-quinazolin-3-yl)-piperidine-2,6-dione, and their pharmaceutical compositions and uses Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed
WO2008079857A1 Crystalline forms of aryl-substituted pyrazole-amide compounds The present invention provides novel crystals of Compound I, pharmaceutical compositions containing such novel form and a method of treating p38 kinase associated conditions, including rheumatoid arthritis, using such novel form.
US20110151028 Topical vaginal preparation A topical pharmacological preparation in the form of cream, suppositories or drops delivered topically to the vagina in order to contract the smooth muscle of the vaginal wall. The preparation contains a smooth muscle contracting agent such as oxytocin capable of constrict the vaginal tube reducing its overall diameter for a more pleasurable sexual experience for the female subject and his partner alike. The smooth muscle contracting agent can be associated with a systemic absorption retardant such as a mixture of Benzyl Alcohol, Acetone and Isopropanol. Such a formulation achieves high local tissue concentration of the smooth muscle contraction substance such as oxytocin in vicinity to the site of application, via minimization of systemic absorption of the smooth muscle contraction inducing substance and at the same time via promotion of its submucosal absorption across the mucosal barrier. As a result of the use of such formulation an increased local smooth muscle contraction activity is expected to occur in the muscularis mucosae.
US20080004342 Fatty acid phenolic conjugates This invention relates to a biologically active formulation containing a conjugate of a fatty acid and a complex phenol. The fatty acid can be selected from a variety of fatty acids including acids have between 12 and 24 carbon atoms. The phenol can be a polynuclear phenol, a polyphenol or a polyfunctional phenol having a variety of substituents. The formulation can include pharmaceutically acceptable carrier, including diluent. The formulation can be provided in an active dosage form suitable to inhibit mammalian cell growth and/or metastasis of malignant cells. The formulation can be used to induce cytotoxicity in mammalian cells particularly tumor cells or to treat and prevent cellular injury or dysfunction.
CN103239627A Medicament for treating skin disease The invention discloses a medicament for treating a skin disease. The medicament is characterized by comprising the following components in parts by weight: 10-20 parts of rhizoma cimicifugae, 10-20 parts of the root of kudzu vine, 10-20 parts of lithospermum, 15-25 parts of dried rehmannia root, 5-15 parts of periostracum cicada, 10-20 parts of ligusticum wallichii and the like. The medicament has the advantages of short course of treatment, good treatment effect, small side effects and the like.
EP1513800A1 N-benzoylureidocinnamate derivatives, method for production and use thereof The invention relates to N-benzoylureidocinnamate derivatives of formula (I), where R1-R11 have the meanings given in the claims, the physiologically acceptable salts and method for production thereof. The compounds are suitable as anti-diabetics, for example.
CN103694165A Gimeracil amorphous cured product and preparation method thereof The present invention provides a method for preparing a gimeracil amorphous cured product. According to the gimeracil amorphous cured product, gimeracil is dissolved in a suitable solvent to make the gimeracil be cured through a certain method so as to form a powdery solid, and the X-ray diffraction detection result shows that at least 90% of the solid exists in the amorphous form. The gimeracil amorphous cured product has good flowability and good bulk density so as to make manufacturing and preparation of the gimeracil-containing drug be easy, can meet preparation process requirements without crushing operation, and has good bioavailability. In addition, the preparation method is suitable for industrial production.
US20120039999 Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists Pharmaceutical compositions of metabotropic glutamate 5 receptor (mGlu5) antagonists or a pharmacologically acceptable salt thereof are disclosed. The compositions contain the therapeutic active compound with non-ionic polymer and ionic polymer, binder and fillers in either matrix pellet, matrix tablet or coated pellets. The compositions provide a pH-independent in vitro release profile with NMT 70% in one hour, NMT 85% in 4 hour, and NLT 80% in 8 hours. The compositions are useful for the treatment of CNS disorders, such as Treatment-Resistant Depression (TRD) and Fragile X Syndrome.
WO2008011007A3 Selective antagonists of a2a adenosine receptors The present invention provides compounds of formulae (Ia) and (Ib): wherein R1-5, Q, X, Y, Z, p, q, and r are as defined herein. The compounds are potent and selective antagonists of A2A adenosine receptors (ARs). The invention further includes pharmaceutical compositions containing these compounds and methods of using the same.
CA2339190C Compressed compositions comprising clarified xanthan gum A solid sustained release pharmaceutical composition comprising a compressed mixture of a pharmacologically active ingredient and a sustained release carrier comprising xanthan gum characterised in that the xanthan gum is capable of dissolving in water at a concentration of 1 part by weight xanthan gum to 100 parts by weight water to form a solution having a transmittance (600 nm) of greater than 50 %. The clarified xanthan gum has an improved reproducibility in drug dissolution.
CN103006615A Soft capsules for treating stomach illness The invention discloses soft capsules for treating stomach illness. The soft capsules comprise liquid medicines and soft capsule shells for sealing the liquid medicines, wherein the liquid medicine comprises active ingredients. The soft capsules can be used for effectively alleviating acute gastritis as well as gastric mucosal lesions (such as erosion, hemorrhage, flushing and edema) in an acute exacerbation stage of chronic gastritis, and also can be used for treating gastric ulcer.
US20100087437 Novel Potassium Channel Blockers The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives wherein R1, R2, R3, X1, and A are defined herein. The compounds are useful as potassium ion channel inhibitors.
US20120329800 Treatment of muscular dystrophies and associated conditions by administration of monoamine oxidase inhibitors Administration of a monoamine oxidase inhibitor is useful in the prevention and treatment of muscle dystrophy. Methods and compositions for inhibiting the production of reactive oxygen species in a muscle cell overproducing reactive oxygen species are provided herein.
CN101209244A Method for producing acetylkitasamycin microcapsule type powder The invention provides a production method of acetylkitasamycin microcapsuled powder, and the microcapsuled acetylkitasamycin powder is obtained by spray drying after mixing 1 part by weight of acetylkitasamycin power and 0.01 to 1 part by weight of cellulose in 10 to 300 parts by weight of organic solvent. The selected cellulose can be ethyl cellulose and methyl cellulose, and the organic solvent can select chloroform, dichloromethane or acetone. The method of the invention can further add non-ionic surfactant in the organic solvent so as to increase the solubility of the drug. In addition, anti-adhesion agent can also be added in the organic solvent, or anti-adhesion powder is added in the microcapsuled finished product, so as to reduce the self-adhesion of the drug and increase the hydrophilic property and solubility of the drug. The production method of acetylkitasamycin microcapsuled powder of the invention has the advantages of improving the dissolution rate of the raw materials and improving the oral bioavailability of the preparation, furthermore, the produced acetylkitasamycin microcapsuled powder is also the powder with the thermodynamic stability.
CN102993195A Substitutional-2-(chroman-6-oxyl) thiazole and application thereof as medicine The invention relates to a substitutional-2-(chroman-6-oxyl) thiazole shown as a formula I, wherein Ar, R2, R3 and R4 are defined in claims. The compound shown as the formula I is a sodium-calcium permutoid (NCX) inhibitor, especially a sodium-calcium permutoid subtype 1 (NCX1) inhibitor, and is applicable to treatment of various disorders caused by calcium unbalance in cells, such as arrhythmia, cardiac failure and apoplexy. The invention also relates to a method for preparing the compound shown as the formula I, an application of the compound as the medicine and a medicine composition containing the compound.
WO2010023946A1 Novel uracil compound having nitrogenated heterocyclic ring or salt thereof Disclosed is a uracil compound having a nitrogenated heterocyclic ring, represented by formula (I), having an excellent inhibitory activity on human dUTPase and useful as an anti-tumor agent or the like, or a salt of the uracil compound. [In the formula, X represents a divalent hydrocarbon which may have a hetero atom between carbon atoms or at the terminal; Y represents H or F; A represents a (substituted) nitrogenated unsaturated heterocyclic ring; and R1 and R2 independently represent H, CN, a (substituted) C1-4 alkyl, a (substituted) C2-4 alkenyl or alkynyl, a mono- or di-alkylaminocarbonyl, an aryl, an unsaturated heterocyclic ring, or a (substituted) aralkyl.]
US20050123551 Nucleic acids encoding polypeptides present in normal and neoplastic endometrial cells for use in diagnosis and treatment of endometrial cancer, identifying endometrial tissue; vectors, host cells; vaccines against endometrial cancer The present invention relates to newly identified nucleic acid molecules and polypeptides present in normal and neoplastic endometrial cells, including fragments, variants and derivatives of the nucleic acids and polypeptides. The present invention also relates to antibodies to the polypeptides of the invention, as well as agonists and antagonists of the polypeptides of the invention. The invention also relates to compositions containing the nucleic acid molecules, polypeptides, antibodies, agonists and antagonists of the invention and methods for the use of these compositions. These uses include identifying, diagnosing, monitoring, staging, imaging and treating endometrial cancer and non-cancerous disease states in endometrial, identifying endometrial tissue, monitoring and identifying and/or designing agonists and antagonists of polypeptides of the invention. The uses also include gene therapy, production of transgenic animals and cells, and production of engineered endometrial tissue for treatment and research.
WO2006040672A1 Substituted cyclopropyl chromene compounds for use in the treatment and prevention of inflammation related conditions The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula (1) Wherein Z, X, R1, R2, R3, and R4 are as described in the specification.
US20130059855 Crystal of di(arylamino)aryl compound Provided are crystals of compound A which have properties suitable for industrial production. MEANS FOR SOLVING As the results of intensive studies to provide crystals of compound A having an inhibitory activity on the kinase activity of an EML4-ALK fusion protein and a mutant EGFR protein, crystals of compound A were found. Moreover, it was found that A04-type crystal of compound A, from among the aforesaid crystals of compound A, unexpectedly have preferred properties as a drug substance.
CN101701217A SiRNA restraining gene expression of transcription factor Spl and application thereof The invention discloses a siRNA restraining the gene expression of a transcription factor Spl, and the length of the siRNA is 16-30bp. The invention also discloses a recombinant carrier which contains the siRNA and transfects host cells by lipofectin transfection, thus obtaining silent cells of the Spl gene. A siRNA array of the invention can effectively degrade the mRNA of the transcription factor Spl gene, thus specifically restraining the expression of the Spl gene. On one hand, the invention can be used for preparing medicines treating diseases related to the Spl gene such as tumor and cell apoptosis related diseases, and on the other hand has important significance on the study of the function of Spl protein in liver cancer and the treatment of liver cancer.
US7198922 Synthesizing polyketide fusion protein comprising acyltransferase domain for use as anthelminthic, insecticide, antitumor, immunosuppressant, fungicidal and/or bactericidal agents A polyketide synthase (“PKS”) of Type I is a complex multienzyme including a loading domain linked to a multiplicity of extension domains. The first extension module receives an acyl starter unit from the loading domain and each extension module adds a further ketide unit which may undergo processing (e.g. reduction). We have found that the Ksq domain possessed by some PKS's has decarboxylating activity, e.g. generating (substituted) acyl from (substituted) malonyl. The CLF domain of type II PKS's has similar activity. By inserting loading modules including such domains into PKS's not normally possessing them it is possible to control the starter units used.
CN1839132A N3-substituted imidazopyridine-derivatives as C-KIT inhibitors Compounds represented by Formula (I): (I) or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
EP1971578A1 21-deoxymacbecin analogues useful as antitumor agents The present invention relates to 21-deoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and / or prophylaxis of cancer or B-cell malignancies.
CN1660754A Ramification biphenyl dienones and application A diphenyldienyl ketone is disclosed, which can be used to prepare medicine for preventing, treating and relaxing the complecations of diabetes.
WO2007104030A1 Retinoids and related compounds for the treatment of neuroinflammatory conditions, diseases and disorders The proliferation and activation of microglia is emerging as an important etiologic factor and target for therapeutic intervention in several CNS diseases including Alzheimer's disease and multiple sclerosis. Here, we have discovered that retinoic acids dramatically inhibit microglial proliferation in an in vivo model including the widely-used animal model of multiple sclerosis, the experimental autoimmune encephalomyelitis (EAE) mouse model.
EP2004165A2 Synergistic combinations of anticancer agents for treating cancer The invention relates to a combination comprising an Erb-B and VEGF receptor inhibitor; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.
CN101272795A Agent for amelioration of insulin resistance Disclosed is a pharmaceutical or beverage/food which can inhibit the production of an adipocytokine, particularly an adipocytokine that can induce the resistance to insulin, to thereby prevent or ameliorate the occurrence of a morbid condition relating to insulin resistance. The pharmaceutical or beverage/food comprises, as an active ingredient, 3-O-beta-D-glucopyranosyl-4-methylergost-7-en-3-ol,or an extract of a plant belonging to the family Liliaceae with an organic solvent or hot water or a squeezed solution of the plant or a fractionated product of the extract or squeezed solution whichcontains the compound.
CN103055323A Capecitabine medicine carrier and preparation method thereof The invention discloses a capecitabine medicine carrier and a preparation method of the capecitabine medicine carrier. According to the capecitabine medicine carrier and the preparation method of the capecitabine medicine carrier, capecitabine is connected with macromolecule with good biocompatibility (BC), two hydroxyl functional groups exist in a cytidine structure in a capecitabine molecule, one of the two hydroxyl functional groups shows certain activity due to small steric hindrance, an esterification reaction occurs between the one hydroxyle functional group and an activated carboxyl compound under alkaline condition when the one hydroxyle functional group is catalyzed through catalyzer, and the capecitabine is connected with an amphipathicity compound in a chemical bonding mode to form an amphipathicity compound with one end hydrophobic and the other end hydrophilic. The amphipathicity compound with one end hydrophobic and the other end hydrophilic can be used for preparation of medicine carrying microspheres or medicine carrying nanoparticles. When the other end of a macromolecular compound connected with medicine is connected with monoclonal antibody (McAb), folic acid, transferring and the like which have tumor targeting functions, the macromolecular compound can leads the medicine to focus on a tumor position, medicine burst release is reduced, released medicine can also be compensated at a medicine release later stage, and the medicine release can be kept at a moderate level for a long time.
US20090192097 Synergistic Herbal Composition from Bacopa Species for Management of Neurodegenerative Disorders and a Process of Preparation Thereof The present invention relates to a potent synergistic herbal composition [BacoMind®] from the plant species Bacopa monnieri and its beneficial effects in learning, memory, cognition and Attention Deficit Hyperactivity Disorder [ADHD] or Attention Deficit Disorder [ADD]. In addition, the present invention provides the synergistic composition derived from Bacopa monnieri such that the resulting composition consists of Bacoside A3 in the range of 0.1 to 25%, Bacopaside II in the range of 0.1 to 25%, Jujubogenin isomer of bacopasaponin C in the range of 0.1 to 25%, Bacopasaponin C in the range of 0.1 to 25%, Bacopaside I in the range of 0.1 to 25%, Bacosine in the range of 0.1 to 25%, Apigenin in the range of 0.05 to 5%, Luteolin in the range of 0.05 to 5% and Sitosterol-D-glucoside in the range of 0.05 to 5% constituting up to 50% by weight of the total composition.
US7423061 Anticarcinogenic agents; tert-butyl 3-{[(2-[(aminocarbonyl)amino]-5-{4-[2-(diethylamino)ethoxy]phenyl}-3-thienyl)carbonyl]amino}piperidine-1-carboxylate This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
US20090143450 Method for treating central pain syndrom or for inducing centrally generated pain in an animal model The present invention provides a method for treating central pain syndrome in a mammal by administering an effective amount of a thalamic anticonvulsant compound. Also provided are methods for inducing centrally generated pain responses in an animal model and for screening and identifying a compound that inhibits T-type calcium channels.
CN102584741A Amides compound, method for preparing same, composition and application thereof The invention relates to the field of pharmaceutical chemistry and pharmacotherapeutics, in particular to a novel amides compound as shown in the following formula (1) and a method for preparing the same, and also relates to an application of the compound in preparing medicines which prevent or cure diabetes mellitus, obesity and metabolic syndrome diseases, as well as a medicinal composition which contains the compound.
CN1944448B Puerarin derivative and its medicinal use The present invention discloses the puerarin derivatives, and their preparation process, medicine compositions and application in preparing medicine for treating cardiac and cerebral vascular diseases, obstruction of retinal artery and vein, sudden hearing loss and other diseases, improving memory and lowering blood sugar.
US20080057054 Controlling activity of telencephalin The invention relates to the field of phagocytosis and more particularly to the field of neurons and neuron diseases. In particular the invention relates to the use of molecules capable of modulating the phagocytosis in neurons, more particularly to molecules modulating the activity of telencephalin.
US8816082 Heterocyclyl-pyridinyl-based biphosphonic acid, pharmaceutically acceptable salt thereof, composition thereof and method of use thereof The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;
CN101006981A Slow released injection containing taxane and platinum Disclosed is a slow release injection containing taxone and/or platinum-group compounds, which comprises slow release micro-balloons and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents selected from taxone and/or platinum-group compounds and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP/TC), p(BHET-EOP/TC), p(BHDPT-EOP/TC), p(BHDPT-EOP/TC), p(CHDM-HOP) or p(CHDM-EOP), copolymer of polyphosphate ester with polylactic acid, Polifeprosan, di-aliphatic acid and sebacylic acid, copolymer or blend of poly(erucic aciddipolymer-sebacylic acid) or poly(fumaric acid-sebacylic acid). The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 40 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.
CN101371835A Medicament composition containing l-rebeprazole and uses thereof The invention provides a drug composition containing rabeprazole which is a pharmaceutically acceptable salt and a compound of solvent of the rabeprazole; meanwhile, the invention also provides an application of the drug composition containing the rabeprazole in maintenance period of curing active duodenal ulcer, benign active gastric ulcer, erosive or ulcerative gastroesophageaal reflux disease (GERD), duodenal ulcer of masculine Helicobacter pylori or erosive/ulcerative gastric-esophagus reflux disease. In the drug composition, the content of the rabeprazole or the pharmaceutically acceptable salt or the compound of the solvent of the rabeprazole is 0.01-99 percent, wherein, 5-200mg of every unit of preparation containing the rabeprazole or the pharmaceutically acceptable salt or the compound of the solvent of the rabeprazole is optimally selected, later 5-100mg of the preparation is further optimally selected, and then 10-50mg of the preparation is again optimally selected.
WO2014159353A1 Solid state forms of vemurafenib hydrochloride Provided herein are solid state forms of Vemurafenib hydrochloride, processes for preparing the solid state forms, as well as pharmaceutical compositions and formulations comprising said solid state forms.
CN102008429A Tacrolimus controlled release preparation and preparation method thereof The invention provides a tacrolimus controlled release preparation and a preparation method thereof. By adopting solid dispersion technology or cyclodextrin inclusion technology or a solubilizing method of adding micronized medicaments into one or more surfactants and the like, the solubility is obviously improved so as to improve the bioavailability; then a framework controlled release preparation is prepared by adding one or more framework materials or a film-controlled or an osmotic pump type controlled release preparation is prepared by coating a controlled release material, and the tacrolimus controlled release preparation is higher in solubility and dissolution rate, high in bioavailability and has controlled release effect. Therefore, the tacrolimus controlled release preparation maintains stable blood concentration, reduces the incidence of an untoward effect, improves the safety of clinical medicaments, is high in yield and low in cost, can realize large-scale industrial production and has obvious economic benefits, the raw materials are readily available and the preparation technology is simple and practical.
CN101199511A Andrographis lactone self-emulsification capsule of antibacterial antiphlogistic The invention provides an andrographolide self-emulsifying capsule with the function of antisepsis and anti-inflammation. The capsule is prepared by the method that 5 percent to 30 percent of the andrographolide, 1 percent to 20 percent of vegetable oil and 1 percent to 40 percent of emulsifier are evenly mixed in the normal temperature; and then 20 percent to 90 percent of solid dispersion forming agent is added into the mixture; then the mixture is heated to reach 60 to 70 DEG C so that the mixture can be mixed evenly by thermal thawing; the mixture is encapsulated into an empty capsule; finally, the encapsulated mixture is cooled. Wherein, the vegetable oil is soybean oil or tea oil; the emulsifier is tween-80, soybean phospholipid or poloxamer 188 ; and the solid dispersion forming agent is polyethylene glycol whose molecular weight is 4000 to 20000.
US20070287931 Methods and systems for administering an appropriate pharmacological treatment to a patient for managing epilepsy and other neurological disorders The present invention provides systems and methods for managing epilepsy. In one embodiment, a method of the present invention characterize a patient's propensity for a future epileptic seizure and facilitates administration of a pharmacological agent. The dosage of the pharmacological agent is typically a function of at least one of the patient's propensity for the future epileptic seizure and time period to seizure.
US20090062303 Deuterium-enriched ziprasidone The present application describes deuterium-enriched ziprasidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN101366868A Medicament composition for preventing birth defect, improving memory and intelligence The invention relates to a medical composition for preventing birth defects and improving memory and intelligence, which comprises Langehead Atractylodes Rhizome, barbary wolfberry fruit, vitamin B complex, and trace elements of zinc and selenium. The medical composition is mainly suitable for pregestational women, pregnant women and wet nurses, is very effective in preventing the birth defects and improving the memory and the intelligence, has both health care and tonic efficacies, and does not generate any side effects even after long-term application.
WO2014047551A1 Flavonoid based antiviral targets The present invention relates to novel compounds for modulating US28 receptor activity and methods for their use in preventing or treating US28 receptor-mediated disorders or conditions.
WO2011039338A3 Use of compounds with sglt-1/sglt-2 inhibitor activity for producing medicaments for treatment of bone diseases Use of compounds with SGLT-1/SGLT-2 inhibitor activity for producing medicaments for treatment of bone diseases The invention relates to the use of compounds with SGLT-1/SGLT-2 inhibitor activity for producing medicaments for treatment of bone diseases like osteoporosis. Preferred is the use of compounds of the formula I in which the radicals have the stated meanings.
WO2010028051A3 Substituted heterocyclic mercaptosulfonamide metalloprotease inhibitors The present invention generally relates to substituted heterocyclic mercaptosulfonamide compounds, precursors, and derivatives as well as methods for the preparation of and pharmaceutical compositions comprising these compounds. These compounds are designed to be potent selective inhibitors of matrix metalloproteinases (MMPs), including, for example, gelatinases, collagenases, matrilysins, metalloelastase, stromelysin, and membrane-type 1 matrix metalloproteinase. These inhibitors may be used for the control of physiological and pathological processes and disease conditions in which MMPs are believed to play significant functions.
US20100222342 Pyrrolopyrazole, potent kinase inhibitors Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.
EP2356105B1 ( pyrrolidin-2 -yl) phenyl derivatives for use in the treatment of pain The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula (I), wherein R1 is (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, or halo(C1-4)alkyloxy; R2 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; R3 is H, (C1-4)alkyl or halo(C1-4)alkyl; R4 is H, (C1-4)alkyl or halo(C1-4)alkyl; R5 is H, (C1-4)alkyl or halo(C1-4)alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C3-6)cycloalkyl group, optionally substituted with halogen; R6 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
WO2012104550A3 INHIBITORS OF THE INTERACTION OF THE SIGMA-1 RECEPTOR WITH hERG FOR USE IN THE TREATMENT OF CANCER The present invention relates to the use of the Sigma-1 receptor (Sig1R) in the context of the post-transcriptional regulation of ion channel membrane expression. The present invention can be used in the field of the treatment of diseases involving ion channels. They are, for example, nervous system diseases, neurodegenerative diseases, heart diseases, and cancer.
WO2012100097A2 Topical minocycline compositions and methods of using the same Topical minocycline compositions with reduced fluorescence are provided. In some instances, the compositions include an amount of a minocycline active agent associated with porous calcium particles. Also provided are methods of using the compositions, e.g., in the treatment of acne.
US20120016338 Chemoablation of tissue using biodegradable, solid salt dosage forms Novel methods for the chemical ablation of tissue (e.g. prostatic tissue) are described. These methods include the steps of: (a) providing one or more solid salt dosage form comprising 50-100% w/w salt; and (b) inserting one or more of such solid salt dosage forms into the tissue. The solid salt dosage form is optionally inserted into the tissue under real-time ultrasonic observation. An advantage of the present invention is its ability to eliminate toxic byproducts. For example, where NaCl-based solid salt dosage forms are used to effect localized chemical ablation, the concentration is ultimately reduced to the level of normal saline (i.e., about 0.9%) upon absorption by the body of the subject being treated.
CN103690575A Oral/applying liquid used for treating stomach and intestine diseases and skin pain Stomach and intestine diseases in the digestive system frequently occur in summer and autumn, and are caused by eating untidy food with shigella dysenteriae. The stomach and intestine diseases are divided into gastroenteritis and deficiency-cold in spleen and stomach according to pathogenic factors. Symptoms of the stomach and intestine diseases comprise uncomfortableness throughout the whole body, watery stool, dyspepsia, paroxysmal stomachache for several times a day, not high fever, pressing pain in the right lower quadrant, and much stool mixed with mucus and rancid flavor. The invention discloses an oral/applying liquid used for treating the stomach and intestine diseases and skin pain. The liquid is prepared by melting 2000 g of fresh quick lime block obtained immediately after a kiln is opened, 3000 g of plain boiled water having a temperature of 85-100 DEG C and a bottle of sesame oil by utilization of a processing technology, and is for oral administration or external local application. Based on clinical pathogenic-factor summary of a plurality of patients and repeated practice, the liquid provided by the invention has strong sterilization functions, disinfection functions, anti-inflammation functions, and skin-care functions. The liquid has unique curative effects for the human stomach and intestine diseases and significant curative effects on the human skin pain, and makes groundbreaking accomplishment for skin protection. The liquid is free of toxic and side effects, and is an innovative technology for treating the stomach and intestine diseases and the skin pain.
US20100247675 Magnotherapy products The present invention relates to a method of treating and/or reducing and/or preventing symptoms associated with menopause comprising applying a magnetic product to a human or animal body wherein the magnetic product comprises a magnet having positive and negative poles, the magnet having a metallic element which distorts the magnetic field distribution around the magnet so as to attenuate the magnetic field in the vicinity of the positive pole of the magnet. The invention also relates to the use of a magnetic product in the prevention and/or treatment of cancer, wherein the magnetic product comprises a magnet having positive and negative poles, the magnet having a metallic element which distorts the magnetic field distribution around the magnet so as to attenuate the magnetic field in the vicinity of the positive pole of the magnet. The invention also relates to the use of a magnetic product to increase the level of IGHBP-3 in a subject, in which the magnetic product comprises a magnet having positive and negative poles, the magnet having a metallic element which distorts the magnetic field distribution around the magnet so as to attenuate the magnetic field in the vicinity of the positive pole of the magnet.
WO2010021750A3 Methods and compositions for administration of 3-halopyruvate and related compounds for the treatment of cancer The present disclosure relates to the discovery that compounds of the invention, particularly 3-bromopyruvate and related compounds, can be safely administered at concentrations effective for the treatment of cancer when formulated with an acidity of greater than or equal to pH of 2 and less than or equal to a pH of 6. Disclosed herein are novel and improved methods and compositions for the treatment of cancer using 3- halopyruvate and related compounds.
CA2551038C Triazole derivatives as vasopressin antagonists Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: V represents a direct link or -O-; Ring A represents an optionally substituted 5- to 7-membered saturated heterocyclic ring, or a phenylene group.
EP1604646A1 Viscous compositions containing carbon dioxide The present invention relates to a carbon dioxide-containing viscous composition comprising an aqueous viscous composition containing one or more thickeners and carbon dioxide, wherein the aqueous viscous composition comprises the carbon dioxide in the form of bubbles, the carbon dioxide-containing viscous composition being characterized in that the thickener is at least one selected from the group consisting of ethyl cellulose, carboxymethyl cellulose and salts thereof, carboxy-methylethyl cellulose and salts thereof, croscarmellose and salts thereof, crystalline cellulose, cellulose acetate, cellulose acetate phthalate, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, hydroxypropylmethyl cellulose phthalate, powdered cellulose, methyl cellulose and methylhydroxypropyl cellulose; a kit comprising a carbonate or carbonates, an acid or acids, a thickener or thickeners and water in a state where the components produce substantially no carbon dioxide, which enables to produce a carbon dioxide-containing viscous composition comprising carbon dioxide bubbles according to the present invention by mixing the carbonate or carbonates, the acid or acids, the thickener or thickeners and water; a pharmaceutical composition comprising, as an active ingredient, the carbon dioxide-containing viscous composition according to the present invention or the carbon dioxide-containing viscous composition obtainable by the kit according to the present invention; and cosmetics comprising the carbon dioxide-containing viscous composition according to the present invention or the carbon dioxide-containing viscous composition obtainable by the kit according to the present invention.
CN103385922A Natural pharmaceutical composition and preparation method The invention relates to a natural pharmaceutical composition and a preparation method. The natural pharmaceutical composition comprises 1, water-decoction condensation extract of cinnamon and myrobalan, 2, cinnamyl aldehyde and 3, 70% ethanol extract of myrobalan according to a ratio of 7-8: 4-7: 2-5. The natural pharmaceutical composition has very good effects on cancer chemotherapy-related diarrhoea and can produce synergism with cancer chemotherapy.
US20080293683 Hormone Replacement Therapy A hormone replacement therapy formulation and method comprising selective estrogenic compounds which preferentially stimulate the estrogen receptor alpha over the estrogen receptor beta.
CA2160016C Method of forming oligonucleotides A method of forming an oligonucleotide is disclosed, the method including the steps of disposing in solution at least two oligonucleotides in aqueous solution wherein one of the oligonucleotides includes an .alpha.-haloacyl group and the other of the nucleotides includes a phosphothioate group and covalently binding the oligonucleotides together through the .alpha.-haloacyl group and the phosphothioate group spontaneously forming a thiophosphorylacetylamino group therebetween.
US20110039854 Linear and cyclic guanidine derivatives, method of preparation and uses thereof The present invention relates to linear and cyclic guanidine derivatives, method of preparation and uses thereof, pharmaceutical compositions to be used as antifungal agents, in particular against Candida species.
US20110195125 Nanoparticles For Drug Delivery To The Central Nervous System The present disclosure relates to compositions and methods for producing nanoparticles to provide relatively more rapid delivery of such particles across the blood-brain barrier. The nanoparticles may be formed from bis-quaternary pyridinium-aldoxime salts that may also be of a specific polymorphic structure and which may be formed in either hydrophobic or hydrophilic type liquid media. In addition, the nanoparticle for transport across the blood-brain barrier may comprise a polymeric resin encapsulating a bis-quaternary pyridinium-2-aldoxime salt of the formula:
EP1328271B1 Treatment of neurological and neuropsychological disorders The present invention discloses a method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression, insomnia, schizophrenia, epilepsy, spasm and chronic pain. Administration of a suitable DP IV inhibitor leads as a causal consequence to a reduced degradation of the neuropeptide Y (NPY) in the brain of mammals. Such treatment will result in a reduction or delay in the decrease of the concentration of functionally active neuronal NPY (1-36). As a consequence of the resulting enhanced stability of the endogenous NPY (1-36), NPY activity is prolonged thereby resulting among other things in functionally active NPY YI receptor activity thereby facilitating antidepressive, anxiolytic, analgesic, antihypertension and other neurological effects.
US20130030018 Tris-Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.
EP1492775A2 Oxo-azabicyclic compounds A compound selected from those of formula (I) wherein: X1, X2, and X3, represent N or -CR3 in which R3 is as described in the description, G1 represents a group selected from those of formulae (i/a) and (i/b) in which R4, R5, and R6 are as defined in the description, G2 represents a group selected from carbon-carbon triple bond, -CH=C=CH-, C=O, C=S, S(O)n1 in which nl represents an integer from 0 to 2 inclusive, or a group of formula (i/c) in which Y1 represents O, S, -NH or -Nalkyl, and Y2 represents O, S, -NH or -Nalkyl, n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, Z1 represents -CR9R10,wherein R9 and R10 are as defined in the description, A represents a ring system, R1 represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d) in which p, Z2, B, q and G3 are as defined in the description and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.
US7087612 Amine oxidase inhibitor; therapy for Alzheimer's diseases, Parkinson's disease This invention relates to 3H-quinazolin-4-one derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as selective monoamine oxidase B inhibitors.
CN101596192B Application of palmatine in medicine for treating dengue virus infection The invention discloses an application of palmatine in medicine for treating dengue virus infection; the inhibition ratio of palmatine to dengue virus (DENV) under the condition that the concentration of the palmatine is 100mu m is 94.95 percent, and the survival rate of Vero cells is 92.93 percent under the condition that the concentration of the palmatine is 100mu m. The palmatine can effectively inhibit proliferation of dengue virus, but has low cytotoxicity, therefore, the palmatine can be further developed into the medicine for treating diseases caused by dengue virus infection and has wide application prospect.
WO2007087518A3 2-substituted benzimidazoles as selective androgen receptor modulators (sarms) The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
CN103209966A Sodium salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide A preparation replete with crystals of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
CN1919219A Refining method of ginko total chromocor and method for preparing ginko damo injection The invention discloses a refining method of ginkgo flavone and preparing method of ginkgo damo injection, which comprises the following steps: adding ginkgo extract in the dimidamo with pH value at 3.0-6.5, setting temperature at 100 deg.c to react, sedimenting at low temperature, hyperfiltering, sterilizing, adopting NaHSO3 as anti-oxidant.
CN1660843A Matrine and salt of organic acid of oxidized matrine and its prepn. process An organic acid's salt of matrine or matrine oxide is prepared from the matrinx or matrine oxide through reacting on organic acid in water and/or organic solvent. It can be used to prepare medicine with high stability and easy absorption.
WO2010131769A1 Treatment of diffuse-type gastric cancers using s-1 and cisplatin The present invention provides an improved method for treating diffuse-type gastric cancer or a mixed-type gastric cancer, including advanced diffuse-type and mixed type gastric cancer and metastatic diffuse-type and mixed-type gastric cancer, by administering S-1 and cisplatin to patients in need of treatment for diffuse-type gastric cancer or mixed type gastric cancer.
WO2012082862A3 Androgen receptor inhibitors and methods of use thereof The present invention relates to novel aryl sulfonamide compounds use of such compounds in the inhibition of angrogen receptor and in the treatment of various diseases, disorders or conditions related to androgen receptor.
DE202006017031U1 Cosmetic or dermatological preparation, useful to treat e.g. skin aging, comprises e.g. vitamin-A, phytosterol, vitamin-E, urea, caprylic/capric triglyceride, lipid, thickener, emulsifier, polymer, perfume, preservatives and water Cosmetic or dermatological preparation (A), comprises: vitamin-A or its biochemical precursors or derivatives (0.02-0.09 wt.%), phytosterol or its biochemical precursor or derivatives (0.1-3 wt.%), vitamin-E or its biochemical precursor or derivatives (0.5-3 wt.%), urea (according to international network of integrated care (INIC) norms) (1-4 wt.%), caprylic/capric triglyceride, lipid, thickener, emulsifying agents, polymers, perfume, preservatives and water. - ACTIVITY : Dermatological. - MECHANISM OF ACTION : Matrix-metalloproteinase inhibitor. The ability of (A) to inhibit matrix-metalloproteinase expression was tested in vitro. The results showed that (A) comprising vitamin A (10-25 mu M) controlled the expression up to 82%.
EP2409700A1 Methods of treatment using intravenous formulations comprising temozolomide This invention relates to methods and drug products for treating proliferative disorders using intravenous formulations comprising temozolomide over a specific infusion time. These methods and drug products are particularly well-suited for patients who cannot swallow oral formulations. These methods and drug products also afford an added convenience to patients who are already receiving other therapeutic treatments.
US20120035154 Modulators of Cellular Adhesion The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
WO2007080560A2 The use of the process of induction of de novo synthesis of p-glycoprotein (p-gp) in the treatment of xenobiotic-induced intoxications in mammals The present invention concerns to the process of induction of de novo synthesis of P-glycoprotein (P-gp) to be used as a treatment of xenobiotic-induced intoxications in mammals and, in particular, of paraquat (PQ)-induced intoxications (Fig. 3). It is shown, for the first time that the induction of de novo synthesis of P-gp, 2 hours after PQ exposure, led to a remarkable decrease of PQ accumulation in the lung to 40% of the group exposed only to PQ, and to an increase of its faecal excretion with the subsequent reversion of the toxicity, as shown by several biochemical and histopathological biomarkers of toxicity in just 24 hours.
WO2009156535A1 Hydrazides of heterocyclic systems and use thereof in the treatment of neurodegenerative diseases The present invention relates to a family of compounds with the structural characteristic of a hydrazide group linked to a heterocyclic system, to pharmaceutical compositions containing same, and to the use thereof as agents for the treatment of diseases of the central nervous system, caused by a series of processes included in what is generically referred to as neurodegeneration.
US7704957 For therapy of AIDS The present invention relates to a composition for inhibiting HIV activity comprising the extract of Paecilomyces sp. (Tochu-kaso) J300. More particularly, the present invention relates to a composition for inhibiting HIV activity comprising 3-[5-(methoxy-ethyl)-3,6-dioxo-piperazine-2-yl]propionic acid represented by Formula 1 and 4-methyl-2-[(pyrrolidine-2-carbonyl)-2-amino]pentanoic acid represented by Formula 2 that are extracted from Paecilomyces sp. (Tochu-kaso) J300; and to a medical composition and food composition containing the same.
US20110142961 Methods and reagents for predicting clinical outcome and customizing chemotherapy in lung cancer patients The invention relates to methods for the prediction of the clinical outcome of a patient suffering from cancer based on the relative expression levels of BRCA1 and RAP80 genes. The invention also relates to anticancer combination therapies comprising a platinum-based chemotherapeutic agent and an inhibitor of RAP80.
WO2014088785A1 Use of telomerase inhibitors for the treatment of myeloproliferative disorders and myeloproliferative neoplasms Provided herein are methods for reducing neoplastic progenitor cell proliferation and alleviating symptoms associated in individuals diagnosed with or thought to have myeloproliferative disorders, such as Essential Thrombocythemia (ET). Also provided herein are methods for using telomerase inhibitors for maintaining blood platelet counts at relatively normal ranges in the blood of individuals diagnosed with or suspected of having myeloproliferative disorders, such as ET.
CA2210684C Use of thiazolium compounds for preventing and reversing the formation of advanced glycosylation endproducts The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositons are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha--dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.
US20080139657 Method for increasing serotonin levels in a person by administration of a composition incorporating (-)hydroxycitric acid, and related compositions thereof A method for increasing serotonin levels in a person includes identifying a person having a deficient serotonin level and administering to the person a composition incorporating hydroxycitric acid, preferably in the form of an extract of Garcinia cambogia, in an amount sufficient to increase the person's serotonin levels. The method also can incorporate administering chromium, preferably in the form of oxygen-coordinated, niacin-bound chromium, and gymnemic acid, preferably in the form of an extract of Gymnema sylvestre, to synergistically work to further increase serotonin levels in the person.
US7304076 Dietetics; antidiabetic agents; eating disorders The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
US20120201748 Coacervate having an ionic polymer mixed with the adhesive protein of a mussel or of a species of the variome thereof The present invention relates to a coacervate comprising a mussel adhesive protein and an anionic polymer, and more particularly, to a coacervate prepared by mixing a mussel adhesive protein with an anionic polymer, and a novel use thereof. In the present invention, a coacervate prepared by mixing a mussel adhesive protein and an anionic polymer shows a very excellent adhesive strength to various substrates such as cells or metals, and is able to maintain its adhesive strength in the presence of water or under water, thereby being effectively used as an adhesive. Moreover, it has an activity capable of encapsulating bioactive materials, thereby being effectively used as an active component of a composition for delivering bioactive materials.
WO2006062097A1 Agent for prevention and/or treatment of pruritus Disclosed is a pharmaceutical agent for prevention and/or treatment of pruritus which contains, as an active constituent, a pyrazolone derivative represented by the formula (I) below, a physiologically acceptable salt thereof, or a hydrate or solvate of those. (I) (In the formula, R1 represents a hydrogen atom, an aryl group, an alkyl group having 1-5 carbon atoms or an alkoxycarbonylalkyl group having 3-6 carbon atoms in total; R2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1-5 carbon atoms, or a hydroxyalkyl group having 1-3 carbon atoms; or R1 and R2 may combine together to form an alkylene group having 3-5 carbon atoms; and R3 represents a hydrogen atom, an alkyl group having 1-5 carbon atoms, a cycloalkyl group having 5-7 carbon atoms, a hydroxyalkyl group having 1-3 carbon atoms, a benzyl group, a naphthyl group, a phenyl group or a phenyl group substituted by 1-3 substituents.)
US7262185 For therapy and prophylaxis of infectious diseases of HIV, in particular, AIDS and is also suitable for oral administration The present invention provides a novel benzazepine derivative represented by formula: wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula —W1—X2—W2— (W1 and W2 are independently S(O)m1 (m1 is 0, 1, or 2), etc., and X2 is an optionally substituted alkylene group etc.), a preparation method and use thereof.
WO2007014498A1 Analgesic huperzine and the derivatives thereof The present invention discloses a method of treating pain, functional painful syndrome or organic painful syndrome, which characterized in using compound of formula (I) and the salts thereof to alleviate or treat the pain, functional painful syndrome or organic painful syndrome in mammals, wherein: R1 represents H or C1-6 Hydrocarbonyl; R2 represents H or C1-6 Hydrocarbonyl; R3 represents C1-6 Hydrocarbonyl, heterocycle group or aryl; R4 represents C1-6 Hydrocarbonyl, heterocycle group or aryl; and R5 represents C1-6 Hydrocarbonyl, heterocycle group or aryl.
WO2012148247A3 Pharmaceutical composition containing oleanolic acid acetate as an active ingredient for preventing or treating tlr- or il-6-mediated diseases The present invention relates to a pharmaceutical composition for preventing or treating TLR- or IL-6-mediated diseases, containing oleanolic acid acetate or pharmaceutically acceptable salts thereof as an active ingredient, and to a pharmaceutical composition for preventing or treating TLR- or IL-6-mediated diseases and containing phaseoli semen extract, or a fraction thereof, which contains said compound or salts as an active ingredient. The phaseoli semen extract or compound according to the present invention is derived from a natural substance, which has long been used in natural medicine, and therefore causes no side effects. The phaseoli semen extract or compound inhibits the activity of TLR-3 and TLR-7 induced by Poly(I:C) and Poly(I), which are the synthetic analogues of dsRNA and ssRNA, blocks signaling pathways including NF-κB, and inhibits the transcriptional activity and phosphorylation of STAT3, which is an inflammation-related transcription factor activated by IL-6. Therefore, the phaseoli semen extract or compound of the present invention can be widely used in developing agents for preventing or treating TLR- and IL-6-mediated diseases, such as atopic dermatitis or arthritis.
CA2200220C Drug for tumor growth suppression The invention relates to the field of biology and medicine, in particular to suppression of the growth of malignant tumors. The object of the present invention is to find more effective and less toxic drugs for suppression of tumor growth. The essence of the proposed invention is that in order to suppress tumor growth, a drug consisting of a biogenic reductant and a complex of cobalt or iron with substituted phthalocyanines (I) or naphthalocyanines (II) is used. (see formula I , II) where R = COONa, SO3Na, CH2C5H5N~C1-, CH2(NH2)2S~CC1-. Use of the proposed drug makes it possible to suppress effectively the growth of a wide range of malignant tumors, in particular to achieve the suppression of proliferation of cancer cells (in vitro), inhibition of the growth of tumors in mice (in vivo) and a substantial increase in their life-span, including that obtained in comparison with use of the prototype.
US20070287689 Therapeutic And/Or Preventive Agents For Chronic Skin Diseases The present invention provides: a therapeutic and/or preventive agent for chronic skin diseases which comprises (a) a phosphodiesterase (PDE)-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) a steroid agent as active ingredients; a therapeutic and/or preventive agent for chronic skin diseases to be administered simultaneously or separately with an interval which comprises (a) a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) a steroid agent, as active ingredients; a kit for treating and/or preventing chronic skin diseases characterized by comprising (a) a first component comprising a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) a second component comprising a steroid agent; and the like.
US20060058320 [1,2,4] Triazolo[1,5-c]pyrimidine derivatives The present invention provides [1,2,4]triazolo[1,5-c]pyrimidine derivatives or pharmaceutically acceptable salts thereof which have adenosine A2A receptor antagonism and are useful for treating and/or preventing a disease induced by hyperactivity of an adenosine A2A receptor, the derivatives being represented by formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents a hydrogen atom, halogen, lower alkyl, lower alkanoyl, aroyl, substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; R3 represents lower alkyl, lower cycloalkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; and Q represents a hydrogen atom or 3,4-dimethoxybenzyl).
US20090169632 Sustained release composition and manufacturing method thereof A sustained release composition comprising a polymer and manufacturing method thereof. The sustained release composition comprises a polymer, a bioactive agent, and a release rate determined agent, wherein the release rate determined agent is dispersed in the sustained release composition to control the release rate of the bioactive agent. The method comprises providing an oil phase comprising a bioactive agent, a polymer, and a release rate determined agent; providing an aqueous phase comprising a surfactant; mixing the oil phase with the aqueous phase to form the sustained release composition having a controlled release effect.
US20080027023 Antiproliferative Compositions Comprising Aryl Substituted Xylopyranoside Derivatives Novel xylose based glycoside compounds that have xylose linked O-, S- or C-glycosidically to an aglycone containing several aromatic rings, and compositions that comprise the novel xylose based glycosides and non-xylose-based anti-tumor agents, pharmaceuticals or dietary supplements. The compounds or compositions are administered to treat proliferative diseases, including various forms of cancer.
US6844363 Storage stability; drugs; influenza therapy Hydrates of the compound of formula (I) and crystalline forms thereof have excellent storage stability and are useful medicaments.
WO2007146085A2 Creatine phosphate prodrugs, compositions and uses thereof Membrane permeable prodrugs of creatine phosphate, pharmaceutical compositions comprising membrane permeable prodrugs of creatine phosphate, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising administering prodrugs of creatine phosphate or pharmaceutical compositions thereof are disclosed. In the Formula (I) wherein: Y and Z are each independently selected from Formula (1), Formula (2), and Formula (3).
US6939853 Administering glucagon-like peptide 1 (GLP-1) compound and an effective amount of an antidyslipidemic drug for therapy of dyslipidemia Methods and uses for treatment of dyslipidemia comprising administration of a GLP-1 compound and another antidyslipidemic drug.
CN101948403A New antibacterial compound The invention relates to a new compound with significant antibacterial activity, the structure is as follows: (formula I), and the new compound has great antibacterial effect for methicillin resistant Staphylococcus aureus (MRSA) and methicillin-sensitive Staphylococcus aureus (MSSA). (Formula I).
EP2412701A1 Novel amide derivative and skin whitening agent Provision of a novel compound having a melanin production suppressive activity and the like. A compound represented by the following formula (I) wherein the symbols are as defined in the description, or a salt thereof, and a whitening agent containing the compound or a salt thereof.
CN102133205A Preparation method of glipizide osmotic pump controlled release tablet The invention relates to a preparation method of a glipizide osmotic pump controlled release tablet. A glipizide tablet core is prepared by the following steps of semipermeable membrane wrapping, laser boring and damp-proof layer wrapping. The preparation method is characterized in that the preparation of the glipizide tablet core comprises preparation of solid dispersoid and preparation of the tablet core. In the preparation method, a solid dispersion technology is utilized, so that the dissolving speed of medicines is improved; the solubility of the glipizide is improved through the fluxing auxiliary materials; and a proper amount of penetration promoter is added to adjust the osmotic pressure so as to achieve constant-speed or approximately-constant-speed release. The invention has the advantages that the process is simple, the cost is low, the release tablet is easy to accept by patients and the treating effect is good.
CN1634063A Externally applied formulation of cetirizine hydrochloride Pharmacological test shows that the externally-used preparation of Cetirizine has ideal allergy resistant and anti-inflammatory action to the rat passive cutaneous anaphylaxis (Rat PCA) model and dimethylbenzene caused mouse otitis model, and also prevents the adverse effect to the central system caused by whole body administration. It is also found in the test, that the externally used preparation of Cetirizine also has very fine inhibitory action to dinitrofluorobenzene caused mouse porphyria hypersensitivity (PTH), the novel pharmacological action of the Cetirizine shows that the Cetirizine external preparation has good therapeutic action to skin inflammations which mainly include porphyria hypersensitivity.
CN101085229A Medicine for treating cerebral thrombus The invention discloses an oral administration medicament for treating cerebral thrombus, which is prepared from root of red rooted saliva, notoginseng, leeches, gastrodia tuber, agkistrodon acutus, astragalus root, musk, batryticated silkworm, earthworm, achyranthes root, Ligusticum wallichii and borneol by a predetermined weight proportions.
US7285664 Heterocyclic or benzenic derivatives of lipoic acid, their preparation and their use as medicaments A compound having a formula selected from the group consisting of wherein the substituents are as defined in the specification. The compounds are useful as intermediates in the preparation of compounds of formula (I), which are useful for inhibiting NO synthase and regenerate antioxidants.
US20120177693 Deep lung pulmonary delivery of treprostinil Administration of aerosolized Treprostinil formulations may provide a more homogeneous lung deposition of treprostinil, whereby making deep lung delivery possible.
WO2014078971A1 Trpv-1 receptor antagonist compound derived from 1,3,4-thiadiazole alkylamides and chalcones This technology comprises compounds derived from 1,3,4-thiadiazole alkylamides and chalcone, which inhibit the activation of the TRPV-1 receptor by means of capsaicin and temperature. Said compounds have a strong antagonist activity in the mode of activation of the TRPV-1 receptor by capsaicin and by temperature. The invention also relates to the use of said compounds in the treatment of diseases wherein the TRPV-1 receptor is overactivated, such as chronic pain.
CN103006602A Quickly-dissolved atorvastatin calcium tablet and preparation method thereof The invention provides a quickly-dissolved atorvastatin calcium tablet and a preparation method thereof. The atorvastatin calcium tablet provided by the invention does not contain surface active agents and alkaline materials, is simple in process, and can be quickly dissolved in the stomach, thereby enhancing the compliance and treatment effect of the administration of patients.
CN101028525B Use of tumor caryon single-antibody in physical therapeutic tumor as synergist An application of the tumor cell nucleus monoantibody as the synergist in physically treating solid tumor by directionally combining with the necrotic tissue of tumor specifically and killing the tumor cells by the nuclein carried by it is disclosed. It features that the normal tissue can not be damaged.
EP1709974A2 Method of treating cardiovascular disease using rapamycin This invention provides a method of treating or inhibiting cardiovascular, cerebral vascular, or peripheral vascular disease in a mammal in need thereof, which comprises providing said mammal with an effective amount of a rapamycin.
CN101822714B Medicine treating psoriasis The invention discloses a medicine treating psoriasis, which comprises the following raw material by weight percent: 20-30g India mustard seed, 0.45-0.55g peppermint oil and 40-60g ethanol. In the manufacture process, at firs the India mustard seed is placed in a container and is heated for obtaining oil in a crucible, the peppermint oil is added and mixed evenly and at last the ethanol is added.The use process is that the skin lesion part is cleaned, dried and coated with the medicine once in the morning and once in the evening. 15 days is a treatment course. Through the clinical trial use,the invention obtains satisfactory efficacy and compared with the similar medicine, the invention has the advantages of quick response, reliable curative effect, small toxic and side effect and the like. The total treatment effective rate reaches more than 98 percent.
US7288517 Especially treating Alzheimer's disease with cetrorelix. The present invention relates to the treatment of dementia and neurodegenerative diseases like Alzheimer's disease with intermediate doses of LHRH antagonists which do not cause a castration. A preferred LHRH antagonist is cetrorelix.
WO2007039781A2 1,2,4-oxadioi.e derivatives with activity at the metabotropic clutamate receptors The present invention relates to new compounds of formula (I) wherein Y1 and Y2 selected from the group consisting of hydrogen, halogen atom; C1-4 alkyl, C1-4 alkoxy, cyano and trifluoromethyl group, Q is -CH- group or N; X1 and X2 are different and are independently selected from N and O; Z is -(CH2)n- group or S; n is 1 or 2; R is selected from the group consisting of optionally substituted C1-7 alkyl, C1-4 haloalkyl, C1-4 hydroxyalkyl, C1-4 cyanoalkyl, C1-3 OC1-3 alkyl, C2-7 alkenyl, C2-7 alkynyl, C0-2(NR1R2)alkyl; an optionally substituted C3-7 cycloalkyl, aryl, heteroaryl or saturated heterocyclyl; R1 and R2 are independently selected from hydrogen, C1-7 alkyl or C1-6 alkanoyl group - and/or enentiomers and/or racemates and/or diastereomers and/or geometric isomers and/or pharmaceutically acceptable salts thereof formed with acids and bases, to the processes for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
CN102670594A Appliance of 4bit-1H-1,2,3- triazole-Beta-lactam derivatives for resisting liver cancer The invention discloses an appliance of 4bit-1H-1,2,3- triazole-Beta-lactam derivatives for resisting liver cancer, wherein the 4bit-1H-1,2,3- triazole-Beta-lactam derivatives have excellent biological activity, have stronger value-added inhibitory activity to liver cancer cells HepG2 shown in testing of in-vitro activity, is a potential anti-cancer drug, and has the appliance for preparing anti-cancer drugs preparation.
CN101167726B Rosiglitazone maleate dispersible tablet and preparation method thereof The invention discloses a new preparation of rosiglitazone maleate: rosiglitazone maleate tablets and a process for preparation, which is made of rosiglitazone maleate 1-20%, disintegration agent 1-70%, bulking agent 10-90%, and lubricating agent 0.1-2%. The invention of rosiglitazone maleate tablets have the advantages of novel preparation, convenient intaking, excellent absorbability, less stimulation on the gastrointestinal tract, stable quality for long-term storage, and especially adapt to the old and the patient with deglutition difficulties. The preparation technique is simple and has no particular requirement on equipment, which adapts to large-scale production. The invention can be used to prepare the medicament for the treatment of II-type diabetes mellitus.
EP2760854A1 Imidazole derivatives as cyp17 inhibitors for the treatment of cancer The present application provides novel imidazole compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP 17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.
WO2008004191A3 Process for the preparation of enantiomerically pure salts of n-methyl-3- ( 1-naphthaleneoxy) -3- (2-thienyl) propanamine The present invention relates to duloxetine salts having enantiomeric purity of 98% or more and a process for such salts.
WO2009037539A3 Treatment of oestrogen dependant conditions in pre-menopausal women The present invention relates to a method for treating and/or preventing ovarian cycle disturbance, prolonged un-opposed secretion of estrogens, and/or ovarian follicular cyst formation in pre-menopausal women with functional ovaries when treated with steroid sulfatase inhibitors (STS-I) for an estrogen-dependant condition.
US7417041 Imidazopyrimidines as transforming growth factor (TGF) inhibitors Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-β signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.
CN101836985A L-pantoprazole magnesium-containing pharmaceutical preparation and preparation method The invention relates to an L-pantoprazole magnesium-containing pharmaceutical preparation and a preparation method thereof. L-pantoprazole magnesium as a main active ingredient and pharmaceutical acceptable excipients are made into the preparation by a certain process, wherein the unit preparation content of the L-pantoprazole magnesium is 10-60mg and is preferentially 20-40mg.
US20130011457 Antimicrobial polymers and methods of manufacture thereof Biodegradable cationic block copolymers are disclosed, comprising a hydrophilic block comprising first repeat units derived from a first cyclic carbonyl monomer by ring-opening polymerization, wherein more than 0% of the first repeat units comprise a side chain moiety comprising a quaternary amine group; a hydrophobic block comprising second repeat units derived from a second cyclic carbonyl monomer by ring-opening polymerization; an optional endcap group; and a chain fragment derived from an initiator for the ring opening polymerization. The cationic block copolymers form aqueous micelle mixtures suitable for antimicrobial applications.
US7087608 Use of PDGF receptor tyrosine kinase inhibitors for the treatment of diabetic nephropathy The present invention relates to the use of PDGF receptor tyrosine kinase inhibitors, especially of N-phenyl-2-pyrim-idine-amine derivatives of formula (I), in which the symbols and substituents have the meaning as defined herein in free form or in pharmaceutically acceptable salt form, in the manufacture of a pharmaceutical composition for the treatment of diabetic nephropathy; to a method of treatment of warm-blooded animals, including humans, suffering from diabetic nephropathy; and to the use of a PDGF receptor tyrosine kinase inhibitor of the formula (I), wherein R1 is pyridyl bonded at a carbon atom, R2, R3, R5, R6 and R8 are each hydrogen, R4 is lower alkyl, R7 a radical of formula (II): —N(R9)—C(═X)—(Y)n—R10, wherein R9 hydrogen, X is oxo, n is 0 and R10 is 4-methyl-piperazinyl-methyl, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for treating glomerulonephritis, chronic pyelonephritis or IgA nephropathy.
WO2012082972A1 Crystalline forms of 5-chloro-n2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-n4[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine The present invention describes specific crystalline forms of 5 -chloro-N-(2-isopropoxy- 5-methyl-4-(piperidin-4-ylphenyl)-N-2-(isopropylsulfonyl)phenyl)-2,4-diamine. The present invention further relates to methods for preparing said crystalline forms, pharmaceutical compositions comprising said crystalline forms, and methods of using said crystalline forms and pharmaceutical compositions to treat disease.
US20100311821 Synthetic vector The present invention includes compositions including a polymer-peptide hybrid and one or more isolated polynucleotides, wherein the polymer of the polymer-peptide hybrid includes a neutral amphiphilic block copolymer, wherein the peptide of the polymer-peptide hybrid is covalently attached to the hydrophobic block of the amphiphilic block copolymer, and wherein the one or more isolated polynucleotides are complexed with the polymer-peptide hybrid via electrostatic interactions between the peptide of the polymer-peptide hybrid and the one or more polynucleotides. The present invention also includes methods of making and using such compositions.
CN102988500A Method for preparing compound Dantong tablets The invention provides a method for preparing compound Dantong tablets. The compound Dantong tablets are prepared from 100g of Dantong, 900g of serrate rabdosia herb, 600g of capillary artemisia, 300g of common andrographis herb and 30g of rhubarb serving as raw medicaments by adopting supercritical extraction and microwave extraction, so that the andrographolide content is greatly improved. The invention also provides application of the compound Dantong tablets in preparation of a medicament for inhibiting propagation of human lung adenocarcinoma SPC-A-1 cells.
CN102357091A Chlocibutamine slow release pharmaceutical composition The invention relates to a chlocibutamine slow release pharmaceutical composition for treating epilepsia and a preparation method thereof. The composition is characterized by containing chlocibutamine and acrylic resin II. The composition of the invention can release chlocibutamine slowly, and a blood drug level has small peak valley fluctuation to avoid toxic and side effect caused by exceeding a treatment blood drug level scope; and the blood drug level can be kept in an effective concentration scope to maintain curative effect and reduce medicine administration times.
EP1863573A1 Treatment of laminitis The present invention provides a composition comprising one or more of a matrix metalloprotease inhibitor, a decarboxylase inhibitor, a fructanase enzyme and/or a flavonoid for use in the prevention of laminitis
US20060142239 Potassium or sodium salt of (-)-2-(4-hydroxyphenyl)ethyl!-thio-3-'4-{4-'(methzlsulfonzl)oxy !phenoxy}phenyl!propanoic acid and their use in medicine A method for the production of a vascular damaging effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer involving a solid tumour, such as colorectal cancer, which comprises one of: the administration of ZD6126 in combination with 5-FU; the administration of ZD6126 in combination with CIT-11; and the administration of ZD6126 in combination with 5-FU and CPT-11. Also claimed are pharmaceutical compositions and kits comprising one of ZD6126 and CPT-11; and ZD6126 and 5-FU and CPT-11. Further claimed is use of one of: ZD6126 and 5-FU; ZD6126 and CPT-11; and ZD6126 and 5-FU and CPT-11, in the manufacture of a medicament for use in the production of a vascular damaging effect in a warm-blooded animal which is optionally being treated with ionising radiation.
CN102038670A Calcium and zinc gluconate oral solution and preparation method thereof The invention discloses a calcium and zinc gluconate oral solution and a preparation method thereof and is characterized in that 54-66g of calcium gluconate, 1.8-2.2g of zinc gluconate, 9-11g of lysine hydrochloride, 1.8-2.2g of activated carbon, 135-165g of sucrose, 10.8-13.2g of lactic acid, 0.9-1.1g of sodium chloride and 0.45-0.55ml of essence are prepared into 1000ml of the oral solution. The calcium and zinc gluconate oral solution provided by the invention has good taste, is uniform and stable, and is beneficial to the absorption of a human body.
WO2007110977A1 Method for treating/preventing disease using cognitive ability of cerebrum and pharmaceutical It is intended to develop a method for fundamentally healing a disease by improving the cognitive ability of the brain. It was found that the cognitive ability of the brain is improved and, consequently, treatment of a given disease including various cancers is possible by using a pharmaceutical for treating or preventing the disease characterized by combining a major tranquilizer and vitamin C or a salt thereof, and if needed, by concomitantly using an infusion, an antidepressant or an iron preparation. It is also intended to provide a method for treating or preventing a disease comprising the step of administrating a major tranquilizer and vitamin C or a salt thereof to a subject with the disease.
EP2727919A1 Benzocycloheptanethiophene derivatives for anti-allergic reactions The present invention provides inhibitors of allergy, and allergic reactions specifically compounds of the present invention are described by the following chemical Formula I: A method for treating an allergic reaction, or allergy diseases or disorders includes administering a therapeutically effective composition comprising a compound of Formula I or a pharmaceutically acceptable salt, solvate or prodrug thereof and a pharmaceutically acceptable carrier, vehicle or excipient to a subject in need thereof.
US7569609 Treating Alzheimer's disease with 2-propylpentanoic acid (valproic acid) or salts thereof; improving the GABAA receptor responses Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7—CH2— or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together is a saturated heterocyclic ring or amino acid residue, R7 is (i) F—(CH2)m- or F3C—CH2—, (ii) alkyl substituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy. Non-toxic and acid addition salts thereof are useful to prevent and/or treat neurodegenerative disease (e.g., Alzheimer's) and neuronal dysfunction by stroke or traumatic injury (e.g., Multiple sclerosis).
CN102885759A Risedronate sodium sustained-release preparation and preparation method thereof The invention relates to a risedronate sodium sustained-release preparation and a preparation method thereof. The risedronate sodium sustained-release preparation comprises 5 to 30% of risedronate sodium, 10 to 60% of one or more chelating agents, 1 to 20% of one or more sustained-release materials and 10 to 70% of other preparation auxiliary materials. The risedronate sodium sustained-release preparation has good treatment effects only through being taken once a week, reduces taking frequency, and improves patient compliance.
WO2007138748A1 Pharmaceutical agent for recovery from fatigue Disclosed is a pharmaceutical agent having an excellent effect of recovering from physical and/or mental fatigue. More specifically, disclosed is a pharmaceutical agent for the recovery from fatigue, which comprises adenosine 5'-triphosphate or a physiologically acceptable salt thereof and a carrot or a processed product thereof.
EP2344505A2 Indole and indoline derivatives and methods of use thereof The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
US20080293631 Treatment for Autoimmune and Inflammatory Conditions The present invention provides methods for preventing the elevation of blood glucose levels, for preventing or delaying the onset of autoimmune and inflammatory diseases or glucose-associated conditions, and for preventing or reducing inflammation in individuals suffering from an autoimmune or inflammatory diseases, the methods comprising administering to subjects in need thereof an effective amount of activated Protein C or precursor Protein C.
US20060106078 Prostamide receptor antagonists The present invention provides prostamide receptor antagonist compounds that may be represented by the general formula I. wherein A, R1, R2, R3, R4 and R6 are as defined in the specification.
EP1853583A1 Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: Chemical formual should be inserted here as it appears on the abstract in paper form. and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non limiting example(s) include, psoriasis), autoimmune diseases (non limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
CN102908352A Application of terazosin or its salt in preparing drug for treating septicemia/stroke The invention relates to an application of terazosin or salt thereof in preparing drug for treating cell apoptosis symptom caused by septicemia/stroke. The applicant discloses that terazosin and salt derivatives thereof have significant effect in inhibiting cell apoptosis. Through septicemia mouse model, ischemic stroke rat model and in-vitro efficacy test on macrophage, it is found that terazosin and salt derivatives thereof have significant pharmacological activity in inhibiting cell apoptosis.
WO2007057508A3 Treatment of pain with a combination of an alpha2 -adrenoceptor antagonist such as atipemezole or fipamezoiie and an opioid receptor agonist, such as tramadol This invention relates to use of an α2-adrenoceptor antagonist for the preparation of a medicament for treating a mammal, including human, to augment the action of a µ-opioid receptor agonist in the treatment of pain, susceptible to treatment with a µ-opioid receptor agonist, and said µ-opioid receptor agonist is a weakly efficacious µ-opioid receptor agonist or a moderately efficacious µ-opioid receptor agonist. This invention also relates to a corresponding method for the treatment or prevention of pain in a mammal, including human. This invention further relates to pharmaceutical preparations. The preparations comprise a weakly efficacious µ-opioid receptor agonist or a moderately efficacious µ-opioid receptor agonist, and a α2-adrenoceptor antagonist.
US20100286124 Prop-2-yn-1-amine inhibitors of monoamine oxidase type b The present invention relates to new prop-2-yn-1-amine inhibitors of monoamine oxidase type B activity, pharmaceutical compositions thereof, and methods of use thereof.
WO2014031487A1 Bivalent inhibitors of iap proteins and therapeutic methods using the same Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.
US20110110868 Functionalized Magnetic Nanoparticles and Methods of Use Thereof The present disclosure provides compositions comprising 2-deoxyglucose-functionalized magnetic nanoparticles. The compositions are useful in various applications, which are also provided.
US20120052125 Cholesteryl Sulfate-Containing Composition As A Haemostatic The present invention relates to a composition comprising a wound dressing device and cholesteryl sulfate and especially to a composition containing cholesteryl sulfate and at least one carrier material for use as a haemostatic agent, as well as to a method for its preparation and use.
US20120288526 Dna sequence and preparation of grass pollen allergen phl p4 by recombinant methods The present invention relates to the provision of the genetic sequence of the major grass pollen allergen Phl p 4. The invention covers fragments, new combinations of partial sequences and point mutants having a hypoallergenic action. The recombinant DNA molecules and the derived polypeptides, fragments, new combinations of partial sequences and variants can be utilised for the therapy of pollen-allergic diseases. The proteins prepared by recombinant methods can be employed for the in vitro and in vivo diagnosis of pollen allergies.
EP1753735A1 Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators The present invention provides substituted thiazole and pyrimidine derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and methods of use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of action of AgRP on a melanocortin receptor and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases which may be responsive to the modulation of melanocortin receptors including obesity-related disorders.
US6989395 TNF inhibitors Compounds of the following backbone structure: which are useful as Tumor necrosis factor (TNF) inhibitors in treating disease related to elevated TNF.
US20080255090 Ceratamines A and B, and Analogues, Syntheses and Pharmaceutical Compositions Thereof Antimitotic compounds and salts are provided in which the compound has the structure (formula (I)): wherein X and Y are substituted or unsubstituted and are selected from carbon atoms and atoms of groups 15 and 16 of the periodic table; Z is selected from N—R, O and S; U is selected from CR1, N, NH, NR, S and O, R1, R2, and R3 are independently selected from H, NH2, NHR, NR2, SH, SR, SiR3, OH, OR, F, CI, Br, I, ═O, ═S and R; W is selected from O, S, and H2; R4 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NR2 and halide; R is selected from H, substituted or unsubstituted aryl, and substituted or unsubstituted 1 to 20 carbon linear, branched, or cyclic, saturated or unsaturated alkyl, in which alkyl carbon atoms are replaced by 0 to 10 oxygen, 0 to 10 sulphur, and 0 to 10 N atoms; and wherein bonds to carbon atoms or to any of X, Y, Z and U are saturated or unsaturated; and providing that when W is H2, R4 is not H, OH, or unsubstituted phenyl.
CN101194894B Dropping pills containing tegaserod maleate and method for preparing the same The invention provides a tegaserod maleate dripping pill and a process for preparation. The invention overcomes the shortcomings of the prior dripping pills that pure natural degrees of findings which are used by the prior dripping pills are not high, and chemosynthesis findings which are commonly used are not in food additives catalogs of some countries, and tastes of the dripping pills are worse. The invention is a pharmaceutical preparation whose natural degree is higher, safety is stronger, and side effect is lower.
CN102846649A Doxycycline hydrochloride for livestock compound injection and preparation method thereof The invention discloses a doxycycline hydrochloride compound injection for livestock and a preparation method thereof, and belongs to the field of drugs for livestock. Per 100mL of the injection mainly comprises the following components, by weight: 5-10 g of doxycycline hydrochloride, 3-5 g of azithromycin, 20-30 g of propylene glycol, 15-25 g of alpha-pyrrolidone, 8-10 g of anhydrous ethanol, 1-2 g of PVP K30, 5-6 g of magnesium oxide, 0.3-0.5 g of sodium formaldehyde sulfoxylate, 3.2-3.5 g of ethanol amine, and the balance of water for injection. According to the invention, doxycycline hydrochloride and azithromycin are compounded to fully play quick-acting antibacterial activity of azithromycin on the basis of realizing long-acting antibacterial effect of doxycycline hydrochloride; drug concentration in body is effectively maintained during the application period, so as to realize efficient, quick-acting and long-acting treatment effect of the drug, and to avoid the inconvenience caused by repeated dosing by veterinary; and the prepared injection has stable quality, and has accurate and fast curative effect on livestock diseases caused by acute moderate and severe infection.
EP2635707A1 Method of examining polycystic kidney disease and method of screening for therapeutic agent of the disease The present invention provides a method of examining polycystic kidney disease or a complication of polycystic kidney disease using a gene(s) selected from the group consisting of NTNG1, POSTN, TNC, KAL1, BST1, ACAT2, INSIG1, SCD, HSD3B1, KRT7, USP40, SULT1E1, BMP6, CD274, CTGF, E2F7, EDN1, FAM43A, FRMD3, MMP10, MYEOV, NR2F1, NRCAM, PCSK1, PLXNA2, SLC30A3, SNAI1, SPOCD1, MMP1, TFPI2, HMGA2, KRTAP4-7, KRTAP4-8, KRTAP4-9, MYPN, RPPH1, and SIAE, and a method of screening for a therapeutic agent or a preventive agent therefore, and further vascular endothelial cells or vascular mural cells obtained via differentiation induction from iPS cells formed from a somatic cell of a subject suffered from polycystic kidney disease and having cerebral aneurysm as a complication.
WO2007002764A3 Di-substituted oxadiazoles as cxc-chemokine receptor ligands Disclosed are compounds of the formula (1). and the pharmaceutically acceptable salts thereof. X is N or N+O-, and Y is N or N+O-, provided that at least X or Y is N. The compounds are useful for the treatment of chemokine-mediated diseases such as COPD.
WO2009129164A1 Pharmaceutical combinations of tfpi-fragments and an antibiotic The present disclosure describes combinations (e.g., pharmaceutical combinations) of anti-bacterial therapeutic agents for the treatment of Gram-positive bacterial infections, e.g., bacterial infections leading to severe pneumonia and/or sepsis. Novel combinations (e.g., pharmaceutical combinations, e.g., pharmaceutical compositions) disclosed herein comprise: 1) C-terminal polypeptides of TFPI in combination with an antibiotic (e.g., vancomycin); and 2) C-terminal polypeptides of TFPI in combination with TFPI or ala-TFPI and an antibiotic. Disclosed herein are methods of using such combinations and compositions for treating Gram-positive bacterial infections, in the manufacture of medicaments for treating such infections, and for reducing cytokine induction by Gram-positive bacteria.
EP2007729A1 Substituted tetrahydroisoquinoline compounds, their preparation and use in medicaments The present invention relates to substituted tetrahydroisoquinoline compounds of general formula (I), a process for their preparation, medicaments comprising said substituted tetrahydroisoquinoline compounds as well as the use of said substituted tetrahydroisoquinoline compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.
WO2007067565A1 Process for the preparation of purified crystalline cci-779 The present invention provides purified crystalline CCI-779 and processes for preparing the same.
WO2010079914A2 A composition comprising the compound isolated from the extract of rubiae radix for preventing and treating inflammatory diseases The present invention is related to the inventive compositions comprising the compounds isolated from Rubiae radix showing potent anti-inflammatory effect through various experiments, therefore, it can be used as the effective and safe therapeutics or health food for treating and preventing inflammatory diseases.
US20100324126 Syn3 compositions and methods Disclosed are aqueous and nonaqueous solution formulations containing agents that are useful for treating cancer.
US20110077212 Therapeutic uses of sglt2 inhibitors Provided are methods of using one or more SGLT2 inhibitors, independently or in combination, for treating edema or reducing fluid retention. The invention also provides methods of using one or more SGLT2 inhibitors for the preparation of a medicament for treating edema or fluid retention. Methods are also provided for treating diabetes with an amount of one or more SGLT2 inhibitors and one or more PPAR-gamma agonists.
CN102603818A Preparation method and use of cerebroside compounds The invention provides a preparation method of cerebroside compounds with a high purify. The preparation method comprises the following steps: smashing Termitomyces albuminosus, performing lixiviation in ethanol, suction filtration and concentration to obtain a crude sample of an ethanol extractum educt, distributing by a solvent, finally obtaining two pure compounds through performing positive and reverse phase silica gel chromatographic column separation and repeated high performance liquid chromatography purification on a normal butanol layer crude sample, and identifying the compounds as cerebroside compounds through spectral analysis. The compounds have new chemical structures, are respectively named as termitomycesphin G (n=16) and termitomycesphin H (n=18), and both have obvious quasi nerve growth factor activities confirmed by experiments. The preparation method is applied to preparation of medicaments for preventing neurodegenerative diseases, such as senile dementia and the like, and is in particular applied to the preparation of the medicaments for treating the neurodegenerative diseases, such as Alzheimer's disease and the like. The chemical structure is as follows.
EP1863777A1 1,2,4 -triazole-5-one compounds as heterocyclic reverse transcriptase inhibitors The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according formula (I) where R1, R2 and R3, are as defined herein.
US20050288353 Methods of modulating c-kit tyrosine protein kinase function with indolinone compounds The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity c-kit kinase.
EP1249450B1 Benzimidazole derivatives as human chymase inhibitors Benzimidazole derivatives of the general formula (1) or medically acceptable salts thereof, being useful as clinically applicable human chymase depressants, wherein R?1 and R2¿ are each hydrogen, alkyl, alkoxy, or the like; A is alkylene or alkenylene; E is -COOR3, -SO3R3, -CONHR3, -SO2NHR3, or the like; G is alkylene; M is a single bond or -S(O)¿m?-; J is heteroaryl; and X is -CH= or nitrogen.
CA2365832C Pharmacological screening of neuronally active substances Pharmacological screening of neuronally active substances is effected by producing second lesion by non-lesion experimental animals by injection in the medial septum of the animal of an amount of vincristine effected by the purpose and administering the substances to be tested by the lesioned animals according to a suitably selected schedule. The effects of the treatment are assessed by evaluation morphological changes, biochemical observation or behavioural observation.
US20120219637 Pharmaceutical compositions of lanthanum carbonate and process for the preparation thereof The present invention relates to compact pharmaceutical compositions of lanthanum carbonate comprising diluents in an amount ranging from about 30% w/w to about 40% w/w of the composition.
WO2005092347A3 Anhydrous pharmaceutical composition associating a siliconated agent and solubilised active principle The invention relates to an anhydrous pharmaceutical composition associating at least one type of active principle and one type of siliconated agent which comprises at least one type of organopolysiloxane elastomer, wherein said active principle is embodied in the solubilised form thereof in said composition.
CN103127089A Application of Eryngiolide A in medicines curing or preventing kidney fibrosis The invention provides application of Eryngiolide A in preparation of medicines curing and preventing kidney fibrosis, and belongs to the medicines new use technical field. New use of the Eryngiolide A in preparation of medicines curing or preventing kidney fibrosis is made public for the first time, due to the fact that the skeleton type is completely novel, and the Eryngiolide A has an unexpectedly kidney fibrosis inhibitory activity. Probability of other compounds giving any revelation for the Eryngiolide A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in preventing and curing kidney fibrosis.
CN103393756A Externally-applied hemorrhoid drug A formula of an externally-applied hemorrhoid drug comprises 30g of Sophora flavescens, 30g of Ficus carica, 30g of river snail, 15g of alum, and 6g of borneol. The preparation method of the externally-applied hemorrhoid drug comprises the following steps: adding water having a mass 2-3 times the total mass of the above five drugs, decocting with water for 30min, and filtering out drug residues to obtain the externally-applied hemorrhoid liquid. Compared with other hemorrhoid treatment methods, the externally-applied hemorrhoid drug has the advantages of convenience, practicality, no pains, no side effects and good effects.
EP1858901B1 Benzothiazole, thiazolopyridine, benzooxazole and oxazolopyridine derivatives as antidiabetic compounds This invention is concerned with compounds of the formula (I) wherein A, B1, B2, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
US7132112 Mixture with alcohol carrier; administering to drug nose mucous membrane; side effect reduction A novel method of vehicle modulated administration of an anticonvulsive agent to the mucous membranes of humans and animals is disclosed. The vehicle system is an aqueous pharmaceutical carrier comprising an aliphatic alcohol (10–80%) or a glycol (10–80%), and their combinations with a biological surfactant such as a bile salt or a lecithin. The pharmaceutical composition provides a means to control and promote the rate and extent of transmucosal permeation and absorption of the medicaments via a single and multiple administration. Nasal administration of the pharmaceutical preparation produces a high plasma concentration of the anticonvulsant nearly as fast as intravenous administration. Such compositions are particularly suitable for a prompt and timely medication of patients in the acute and/or emergency treatment of status epilepticus and other fever-induced seizures.
WO2010032154A3 Gangliosides from the avian nervous system and their uses for the diagnosis and the treatment of proventricular dilatation disease A ganglioside or a mixture of gangliosides, isolated from the peripheral and central nervous system of a bird, in particular a parrot, their use for the preparation of a medicament, methods for the diagnosis of Proventricular Dilatation Disease and diagnostic kits thereof, are disclosed.
CN103301330A Medicinal liquor for treating hematochezia The invention provides medicinal liquor for treating hematochezia. The medicinal liquor is characterized by being prepared from the following raw materials in parts by weight: 40-60 parts of radix sanguisorbae, 40-60 parts of cogon grass rhizome, 30-40 parts of red peony root, 20-30 parts of liquorice, 30-40 parts of manyprickle acathopanax root, 30-40 parts of cactus, 200-300 parts of white sugar and 400-600 parts of rice wine. During preparation, the radix sanguisorbae, cogon grass rhizome, red peony root, liquorice, manyprickle acathopanax root and cactus are mashed and are put into a cloth bag, the cloth bag is put into a container, the rice wine is added, the materials are cooked for one hour in a waterproof manner, the white sugar is added, and the liquor is filtered to remove dregs after the materials are soaked for three days, thus obtaining the medicinal liquor. When in use, about 20-30ml of the medicinal liquor is taken each time and is orally taken twice a day on an empty stomach. The medicinal liquor is reasonable in compatibility, is convenient to use, can cool and stop blood, and can effectively treat hematochezia, hematuria and the like.
CN101190227A Betamethasone chewable tablets for dog or cat The invention discloses a betamethasone chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the existing tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 5 to 20 percent of betamethasone.
US20100087426 Process and intermediates for the synthesis of 8-[-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations.
US20100204259 Immediate release composition resistant to abuse by intake of alcohol The present invention provides immediate release pharmaceutical compositions for oral administration that are resistant to abuse by intake of alcohol.
WO2010065491A3 Methods of treating inflammatory disorders Disclosed herein, in certain embodiments, are methods and compositions for treating inflammatory disorders. In some embodiments, the methods comprise co-administering synergistic combinations of modulators of inflammation.
WO2012129262A1 Treatment of attention deficit/hyperactivity disease The present invention relates to methods and uses for 2S,3R)-N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide or a pharmaceutically acceptable salt thereof.
WO2009120789A1 Bicyclic nitroimidazoles covalently linked to substituted phenyl oxazolidinones The current invention provides a series of bicyclic nitroimidazole- substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild- type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.
CN101513477A Analgesic medicine for external application and method for preparing same The invention discloses an analgesic medicine for external application and a method for preparing the same. The analgesic medicine for external application is prepared from raw materials of realgar, frankincense, myrrh, natural indigo, borneol, fructus kochiae, magnolia bark, angelica dahurica, mirabilite, dragon's blood, alum and camphor through screening, washing, drying in the sun, pulverizing and sieving and according to a weight ratio of 1-2:1 of medicinal powder to table vinegar. The analgesic medicine for external application is mainly applied to relieving pains of late liver cancer, lung cancer and rheumatism, and the total effective ratio for treating the pains of the liver cancer, the lung cancer and the rheumatism is 96.6 percent. The analgesic medicine for external application is not addictive with low price.
EP1228072B1 Pdgf receptor kinase inhibitory compounds, their preparation, purification and pharmaceutical compositions including same A preparation of a tyrphostin including a compound of a general formula (Compound I) or (Compound II), wherein, for (Compound I), the preparation is enriched either for R6 at position 6 or for R6 at position 7, or, for (Compound II), the preparation is enriched either for R6 at position 6 or for R6 at position 8.
WO2008081266A1 Compounds for the treatment or prevention of infection by flaviviridae The present invention provides compounds, pharmaceutically acceptable derivatives thereof and pharmaceutical compositions that are useful as Flaviviridae replication inhibitors.
WO2008021309A1 Imidazolidin-2-one derivatives useful as pr modulators Compounds of structure (I) are described, wherein R1-R6, R10, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
CN101579310A Decataxel self-microemulsifying composition and preparation method thereof The invention belongs to the field of medicinal preparations, and relates to a decataxel self-microemulsifying composition for injection and a preparation method thereof. The decataxel self-microemulsifying preparation comprises the following components by weight percentage: 1 to 20 percent of decataxel, 5 to 60 percent of oil phase, 10 to 90 percent of emulsifier, 1 to 30 percent of coemulsifier, and 0 to 10 percent of additive. The preparation method comprises the following steps: mixing the decataxel, the oil phase, the emulsifier, the coemulsifier and a stabilizer; performing ultrasonic treatment; stirring the mixture at a temperature of between 20 and 80 DEG C to ensure that the mixture is completely dissolved; and mixing evenly to obtain the composition. The self-microemulsion can be directly used and can also be diluted into products of any steady concentration to use by adding the moisture in any proportion. The composition reaches a human body through injection or oral administration, can spontaneously form a microemulsion with nanometer particle size when encountering body fluid, obviously improve the solubility of medicaments, increase the stability of the medicaments, and improve the bioavailability. The composition has the advantages of simple preparation process, high production efficiency, steady product quality, and easy industrialized large-scale production.
CN1772075A Health article (or medicine) applied externally to penis for improving and treating impotence and prospermia The present invention is health article (or medicine) applied externally to penis for improving and treating impotence and prospermia. The health article (or medicine) for prospermia is prepared through soaking tortoise plastron, opium poppy hull, etc in alcohol; and health article (or medicine) for impotence and prospermia is prepared through soaking tortoise plastron, stramonium flower, etc in alcohol. The present invention is suitable for all the patients, and has low cost.
CN101617827B Supramolecular composite of isosteviol or derivative thereof and preparation method thereof The invention relates to a supramolecular composite of isosteviol or a derivative thereof and a preparation method thereof, and the form thereof is a white solid inclusion compound. The mass ratio of the isosteviol or the derivative thereof in the composite to beta-cyclodextrin (or the derivative thereof) is 1:3.57-1:107.1, namely the content of the isosteviol or the derivative thereof of the composite is 0.925%-21.88%; and the solid inclusion composite is the white solid composite prepared by mixing the isosteviol or the derivative thereof with the beta-cyclodextrin in the presence of water.The preparation method of the composite comprises the steps of adding the isosteviol or the derivative thereof with the mass (dry mass) of 1/3.57-1/107.1 into water solution or suspensoid of beta-cyclodextrin, mixing, grinding or carrying out ultrasonic treatment, cooling, filtering, obtaining a solid matter and vacuum drying for preparation to obtain the product in the invention, and the preparation method does not need to add any organic solvent during the preparation process. The composite features good solubility and easy processing, thereby being a good health care food or drug raw material.
CN103505454A Alpha-tubulin inhibitor and application thereof The invention discloses an alpha-tubulin inhibitor and application thereof. The active ingredients of the alpha-tubulin inhibitor consist of effective quantities of at least one lactone compound of alantolactone, isoalantolactone, dihydro-alantolactone, dehydrocostunolide lactone, costunolide and dihydro-costunolide. The alpha-tubulin inhibitor disclosed by the invention can obviously inhibit alpha-tubulin and the mRNA (Messenger Ribonucleic Acid) level thereof, can inhibit the forming of spindles, block the cell cycle in the G2/M period, induce cell apoptosis and the like, can effectively inhibit the tumor growth speed, can obviously inhibit growth of various tumor cells, particularly has an obvious effect on melanoma, can be expected to be used for preparing medicament preparations for resisting tumors and has wide application prospect, wherein the tumors comprise lung cancer, pancreatic cancer, prostatic cancer, neuroblastoma, melanoma and breast cancer.
CN101401822A General medicinal powder for treating beriberi, foot corn and callus on the sole The invention discloses general medicinal powder for treating dermatophytosis, corn and callus. The general medicinal powder consists of the following components which are ground into medicinal powder in weight portion: 100 portions of salicylic acid, 0.1 to 10 portions of calomelas, 0.1 to 9 portions of centipede and 0.1 to 9 portions of potassium permanganate. The components of the salicylic acid, the calomelas, the centipede and the potassium permanganate contained in the medicinal powder are cooperated with each other for sterilization, disinfection, oxidation, itching relief and pain relief. The invention provides a patient suffered from toe-sole diseases such as the dermatophytosis, the corn, the callus and the like with the general medicinal powder capable of quickly relieving itching, relieving the pain and strengthening the curing effect. The general medicinal powder has the advantages of scientific and precise formula, reliable effect, no side effect, slow action, reliable effect, low recurrence rate, 100 percent of effective rate and 100 percent of curing rate.
US20080113965 Skeletal muscle protecting agent The present invention provides a novel drug which is useful as a skeletal muscle protecting agent comprising a compound having inhibitory activity against squalene synthase or a salt thereof, or a prodrug thereof.
EP2749284A2 Combination of glycopyrronium and carmoterol The present invention relates to pharmaceutical compositions for inhalation comprising glycopyrronium and carmoterol; to a process for preparing such compositions and to the use of such compositions for the prevention and/or treatment of respiratory, inflammatory or obstructive airway disease.
CN101361813A Rhubarb eyedrops The invention discloses a rhubarb eyedrop which is prepared by boiling 5 portions to 15 portions of rhubarb and 1000 portions of water by weight. The eyedrop has accurate curative effects and high cure rate. The rhubarb has functions of clearing away heat and toxic material, anti-inflammatory, and activating blood circulation to dissipate blood stasis, and has good curative effects of bacterial and virus inflammation with the cure rate of 100 percent. By the adoption of the rhubarb eyedrop, electric ophthalmia can be cured in 6 hours to 12 hours so as to solve the difficulty that no drug is used for the treatment of the electric ophthalmia, and has quick acesodyne. The rhubarn eyedrop has quick curative effects and acute conjunctivitis, and chronic conjunctivitis can be cured in 1 day to 3 days with simple preparation method and low cost.
US20080070974 4-((1E)-2-(((E)-2-fluoro-4-cyanostyrylsulfonyl)methylsulfonyl)vinyl)-3-fluoro-benzonitrile; mitogen activated protein kinase inhibitor; cell growth factor receptor antagonist; angiogenesis inhibitor, antiproliferative and anticarcinogenic agent; neurodegenerative diseases α,β-Unsaturated sulfones, sulfoxides, sulfonimides, sulfinimides, acylsulfonamides and acylsulfinamides of Formula I: wherein R1, R2, M1, M2, L, E1, E2, Q1, Q2 and n are as defined herein, are useful as anti-angiogenesis agents, as agents for treatment of age related senile dementia, and as antiproliferative agents including, for example, as anticancer agents.
WO2012143041A1 Composition, method for its manufacture and use thereof A composition, a method for its manufacture and uses thereof is disclosed.
CN101600427A Use of substituted pyranone acid derivatives for the treatment of metabolic syndrome The invention relates to the use of substituted pyranone acid derivatives and their physiologically acceptable salts for producing medicaments for the treatment of metabolic syndrome. The invention also relates to the use of compounds of formula (I), in which the radicals are defined as cited in the description, and their physiologically acceptable salts for producing a medicament for the treatment of metabolic syndrome.
WO2011040166A1 Oral composition for reducing wrinkle formation Provided is a novel composition that acts to inhibit and/or ameliorate wrinkle formation, does not have adverse effects like those of retinoids, and is highly photostable. An oral composition for reducing wrinkle formation and an oral composition for preventing wrinkle formation are provided, said compositions containing at least one compound selected from a group comprising D-glutamic acid and derivatives and/or salts thereof. Also provided are a pharmaceutical composition and a food composition containing the aforementioned oral composition for reducing wrinkle formation or the aforementioned oral composition for preventing wrinkle formation.
CN102100822A New application of pure safflower oil The invention provides new application of pure safflower oil. Chilblain is treated by using the pure safflower oil. The pure safflower oil is applied to a skin surface layer on which chilblain positions occur and is rubbed by hands until the chilblain positions are hot, the pure safflower oil is applied for 1 to 2 times a day, and the chilblain can be cured generally within 3 to 7 days and gets better obviously within 1 to 4 days. The pure safflower oil is irritant to damaged skin, so the new application of the pure safflower oil for treating the chilblain is not suitable for treating patients who suffer from skin damage, and for the patients who suffer from the skin damage due to the chilblain, after the damaged skin is cured, a treatment method of the pure safflower oil is used.
WO2014143051A1 Fluorinated pyrimidine analogs and methods of use thereof Fluorinated pyrimidine analog compounds, compositions that include the fluorinated pyrimidine analog compounds, methods for making the fluorinated pyrimidine analog compounds, and methods for inhibiting DNA methyltransferase, treating solid tumors, and treating hematologic cancers by administering the fluorinated pyrimidine analog compounds.
US20100249122 Kinase Inhibitors for Preventing or Treating Pathogen Infection and Method of Use Thereof The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.
CN102048722A Divalproex sodium sustained-release tablet and preparation process thereof The invention provides a method for preparing a divalproex sodium-containing sustained-release tablet for treating epilepsy. The sustained-release tablet contains divalproex sodium, a sustained-release material, a binder and a lubricant. The preparation method comprises the following steps of: mixing the divalproex sodium and the sustained-release material to obtain a mixture, adding the binder for wet granulation, drying, granulating, adding into other uniformly mixed auxiliary materials, and tabletting to obtain the divalproex sodium-containing sustained-release tablet. The sustained-release tablet can be sustainedly released for 24 hours, and is good in appearance, stable in performance and convenient to take.
CN101683527A Compound preparation for treating cold and preparation method thereof The invention relates to a compound preparation for treating cold and a preparation method thereof, belonging to the technical field of medicines. The compound preparation contains a sustained-releasedosage form prepared by respectively selecting an ingredient from an adrenomimetic drug and an antipyretic-analgesic and anti-inflammatory drug, and a fast-release membranous layer formed by any ingredient of an antihistamine drug, wherein the membranous layer is coated on the sustained-release dosage form, the antihistamine drug has fast effect and long time of drug effect, better treating effect can be achieved by fast release of the fast-release membranous layer, and simultaneously, the constant drug level of the adrenomimetic drug and the antipyretic-analgesic and anti-inflammatory drug is maintained in blood by sustained-release releasing. Therefore, the compound preparation can overcome the symptoms related to the cold, including the symptoms of nasal obstruction, sneeze, nasal bleeding, sputum itching, lacrimation and the like with pain and fever.
CN103316040A Rehydration method of piglet diarrhea rehydration salts The invention relates to a rehydration method of piglet diarrhea rehydration salts. Piglets are divided into two day age groups which are respectively supplemented with the rehydration salts, the first day age piglets are supplemented with a first rehydration salt in an intraperitoneal injection manner, and the second day age piglets are supplemented with a second rehydration salt in a drenching or free water drinking manner. The first day age group is piglets of seven or below day ages, and the second day age group is piglets of above seven ages. In the invention, the piglets are divided into two day age groups according to the body growth differences of the piglets of different day agents and are supplemented with different rehydration salts to ensure the rehydration effect, so the rehydration method of piglet diarrhea rehydration salts decreases the labor operating strength and increases the maneuverability of the rehydration method. The rehydration method of piglet diarrhea rehydration salts has the effects of piglet body electrolyte and acid-base balance maintenance, energy supplementation, stress resistance, anti-inflammation and vomiting prevention.
US20060293335 Riboflavin derivative and its manufacture and uses The invention discloses riboflavin derivatives, and a process of preparing the same, and their applications. The w/o suspending preparation of the riboflavin derivatives has high stability, and the effects could last for 3 months after intramuscular injection at dose of 150 mg. This invention increases significantly the bioavailability of riboflavin in vivo, and provides an important treatment method for cure of ariboflavinosis. The preparation is found to have remarkable effect on dermatitis, oral and digestive tract catarrhs caused by bone marrow transplantation for leukemia and chemotherapy for tumor. It is also found to have noticeable effect on persistent oral ulcer, and enhance the tolerability to chemotherapy and radiotherapy. In the treatment of coronary heart disease and hypertension syndrome, arthritis and burn wound, the preparation also has significant effects. This invention has a wide application perspective for its simple techniques, definite long-acting action and effectiveness.
WO2009088860A3 A method of preventing contrast-induced nephropathy The present invention relates to methods of preventing contrast-induced nephropathy including the step of administering an effective amount of a compound (e.g., a peroxynitrite decomposition agent, a PARP inhibitor or a superoxide dismutase mimic) to a subject to be administered a contrast agent.
US20100092427 Pyridinone Diketo Acids: Inhibitors of HIV Replication in Combination Therapy A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HTV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described. Compounds of the present application include those of formula I and include tautomers, regioisomers, geometric isomers, and pharmaceutically acceptable salts thereof, wherein the pyridinone scaffold and R groups are as otherwise defined in the specification. These are combined, with any number of typical other anti-HIV agents (including other integrase-based anti-HIV agents) and other combination therapeutic agents described herein, to provide an effective treatment modality for HIV infections, including AIDS and ARC.
CN103319431A 2-mercaptoacetophenone-containing 1, 3, 4-oxadiazole derivative, its preparation method and antitumor activity The invention relates to a 2-mercaptoacetophenone-containing 1, 3, 4-oxadiazole derivative, which is characterized by having a general formula as the following. In the formula, R1 represents the following, and R2 represents -H -Br. The 2-mercaptoacetophenone-containing 1, 3, 4-oxadiazole derivative provided in the invention has an inhibiting effect on MCF-7 and A431, and has a strong inhibitory effect on A431. Therefore, the 2-mercaptoacetophenone-containing 1, 3, 4-oxadiazole derivative disclosed in the invention can be a potential antitumor drug. The invention also discloses a preparation method of the 2-mercaptoacetophenone-containing 1, 3, 4-oxadiazole derivative.
CN102258531B Medicinal composition containing adenosine cyclophosphate and meglumine and preparation method thereof The invention provides a medicinal composition containing adenosine cyclophosphate and meglumine and a preparation method thereof. The medicinal composition comprises adenosine cyclophosphate serving as an active ingredient, meglumine serving as a stabilizer and mannitol serving as a skeleton in a certain mixing ratio. The composition minimizes the degradation of adenosine cyclophosphate and therefore protects the stability, effectiveness and safety of the medicines.
WO2013053942A1 4-amino-3-phenylamino-6-phenylpyrazolo[3,4-d] pyrimidine derivatives, their manufacture and their use as antiviral active substances The present invention relates to 5-amino-3-pheylamino-6-phenylpyrazolo[3,4-d] pyrimidine derivatives of the general formula (I) or pharmaceutically acceptable salts or prodrugs thereof, wherein at least one hydrogen atom is replaced in at least one of phenyl groups A and B by a substituent RH, which has a Hammett constant σp greater than 0.23. The present invention further relates to a method of manufacturing these. Corresponding compounds have been found to have surprisingly high activity against viruses, particularly rhinoviruses and picornaviruses. Moreover, the compounds are very well tolerated. For these reasons, the compounds are suited for the treatment of viral infections and as medications.
WO2008096690A1 Polyethylene glycol derivative Disclosed are: a novel polyethylene glycol derivative; a drug carrier comprising the derivative; and a pharmaceutical composition comprising the drug carrier having a pharmacologically active substance included therein. Specifically disclosed are: a polyethylene glycol derivative represented by the general formula (I); a drug carrier comprising the derivative and 2-O-(2-diethylaminoethyl)carbamoyl- 1,3-O-dioleoyl-glycerol; and a pharmaceutical composition comprising the drug carrier and a pharmacologically active substance (preferably double-stranded RNA, double-stranded DNA or an oligonucleic acid). Wherein R represents a saturated or unsaturated aliphatic hydrocarbon group having 10 to 30 carbon atoms or a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms; and n represents an integer of 30 to 150.
WO2007004958A1 Pyridopyrimidine derivatives as pde4 inhibitors for the treatment of inflammatory and' immune diseases The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.
WO2014003411A1 Method for preparing α-crystalline form of imatinib mesylate The present invention provides a method for preparing the α-crystalline form of imatinib mesylate. The method of the present invention may involve using a mixed solvent as a reaction solvent to significantly reduce the content of isopropyl alcohol remaining in the α-crystalline form of imatinib mesylate ultimately obtained.
US20080194672 Growth hormone secretagogue (ghrelin) receptor; gastrointestinal disorders; gastroesophageal reflux disease (GERD), gastric ulcers, Crohn's disease The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
US20130023577 COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION OF Eg5 AND VEGF GENES This invention relates to compositions containing double-stranded ribonucleic acid (dsRNA) in a SNALP formulation, and methods of using the compositions to inhibit the expression of the Eg5 and Vascular Endothelial Growth Factor (VEGF), and methods of using the compositions to treat pathological processes mediated by Eg5 and VEGF expression, such as cancer.
DE102004037885A1 New cage dimers of 4-phenyl-1,4-dihydropyridine derivatives, useful as HIV-1 protease inhibiting anti-HIV agents and for increasing resorption and bioavailability of other anti-HIV drugs Symmetrical cage dimers (I) of 3,5-bis-(hydroxymethyl)-4-phenyl-1,4-d ihydropyridines are new. Symmetrical cage dihydropyridine dimers of formula (I) are new. R1>H, alkyl, aryl, alkoxycarbonyl, aryloxycarbonyl, alkylcarbonyl or arylcarbonyl; X : H, OH, CH2OH or NH2. An independent claim is also included for the preparation of (I). [Image] - ACTIVITY : Anti-HIV. - MECHANISM OF ACTION : HIV-1 protease inhibitor. A symmetrical cage dimer of formula (Ia) exhibited a Ki value of 600 nM for the inhibition of HIV-1 protease.
US6855729 Such as the racemic substance RS pindolol The present invention provides a method for treating fibromyalgia and/or chronic fatigue syndrome by administering an antagonist or partial agonist of 5HT1a receptors.
EP2408306A1 Substituted nucleoside and nucleotide analogs Disclosed herein are nucleotide analogs with protected phosphates, methods of synthesizing nucleotide analogs with protected phosphates and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with protected phosphates.
WO2014107535A1 Boronic acid derivatives and therapeutic uses thereof Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents. Other embodiments relate to pharmaceutical compositions containing boronic acid derivatives and additional excipient such as meglumine.
CN101953791A Capsule containing cefprozil liposome and preparation method thereof The invention relates to a cefprozil liposome and a preparation method thereof as well as a capsule containing the cefprozil liposome. The cefprozil liposome comprises cefprozil, hydrogenated yolk lecithin, soyabean lecithin, cholesterol and vitamin E, wherein the weight ratio of the cefprozil to the hydrogenated yolk lecithin to the soyabean lecithin to the cholesterol and to the vitamin E is 1:(1.25-5):(1.25-5):(2.5-10):(0.1-3). The cefprozil capsule not only meets the Chinese pharmacopoeia requirement but also has the advantages of higher dissolution rate, faster action of medicament effect and obvious improvement of bioavailability compared with those of a common cefprozil pharmaceutical composition.
CN102525928A Cis-platinum long-cycle liposome and preparation method thereof The invention relates to a cis-platinum long-cycle liposome and a preparation method thereof, mainly solving the problem that cis-platinum is high in toxicity and a cis-platinum liposome is low in drug loading capacity. The preparation of the liposome depends on the electrostatic acting force between phosphatidyl glycerol derivates with negative charges and hydrate cis-platinum with positive charges. The cis-platinum long-cycle liposome disclosed by the invention can be controlled to be about 120nm in particle size, has higher encapsulation efficiency and drug loading capacity as well as better stability, and is simple and feasible in the preparation method.
CA2410387C Polymerizable compositions and methods of use The present invention provides compositions comprising a first component and a second component, wherein the first component includes at least two polymerizable organic monomers, and wherein the second component includes an oligomer of a polymerizable organic monomer, a plasticizer and an opacificant agent, wherein said composition polymerizes upon contact with an anionic environment. The compositions are useful for filling, occluding, partially filling or partially occluding an unfilled volume or space in a mass in an anionic environment. The composition are also useful for ablating diseased or undesired tissue by cutting off the blood supply to the tissue.
WO2009089093A1 Thyroid hormone receptor agonists The present invention provides for dosage amounts and uses for 2-(4-(4-hydroxy-3- isopropylbenzyl)-3,5-dimethylphenoxy)acetic acid, or a pharmaceutically acceptable salt thereof agents in the treatment of disease states which are alleviated by treatment with a thyroid hormone receptor agonist. Also provided are unit dosage forms comprising 2-(4-(4- hydroxy-3-isopropylbenzyl)-3,5-dimethylphenox)acetic acid.
CN103110625A Azlocillin sodium drug composition and preparation method thereof The invention provides an azlocillin sodium drug composition and a preparation method thereof, relating to the fields of pharmaceutical preparations and preparation methods and mainly solving the problems that single preparations of azlocillin sodium and metronidazole in the prior art have great dosages, poor treatment effects after being combined and big side effects. The drug composition comprises azlocillin sodium and metronidazole lipid microspheres in a weight ratio of (100:3)-(100:10), wherein the weight of the metronidazole lipid microspheres is based on metronidazole. The drug composition is prepared into powder injection. The pH value of water solution of the drug composition is 6.5-7.0. The powder injection of the drug composition provided by the invention not only has high curative effect but also can reduce the dosage of metronidazole by over 80%, thus greatly reducing or avoiding the toxic and side effects, especially gastrointestinal reactions including nausea, emesis, anorexia, abdominal cramp and neurotoxicity, of metronidazole and further reducing the occurrence rate of adverse reactions.
WO2007100295A1 Novel dual action receptors antagonists (dara) at the ati and eta receptors The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.
US20100316631 Water Soluble Curcumin-Based Compounds The present disclosure describes the design and synthesis of a novel class of water soluble curcumin-based compounds. These water soluble curcumin-based compounds are shown to provide superior cell killing activity and exhibit increased and cell internalization solubility in aqueous solutions as compared to the free (unconjugated) curcumin. The present disclosure provides compositions for the treatment or prevention of a variety of disease states or conditions, such as but not limited to, cancer, other cell hyperproliferative disorders and chronic inflammatory conditions, said compositions comprising a water soluble curcumin-based compound.
US20100086518 Treatment of melanoma Methods of treating melanoma include administering a compound of Structure I, a tautomer of the compound, a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable salt or the tautomer, or a mixture thereof to a subject. The compound, tautomer, salt of the compound, salt of the tautomer, or mixture thereof may be used to prepare medicaments for treating metastatic cancer. The variable A has the values defined herein.
WO2010111171A3 Enhanced treatments to kill or debilitate pathogenic microorganisms of a mammalian body Present invention relates to a composition of matter and a method that improves treatments to inactivate, kill and debilitate pathogenic microorganisms that infect on or within a mammal body, such as Helicobacter pylori. The composition of matter comprises anti-adhesive polysaccharide molecules to abolish or reduce the adhesion of H. pylori to themselves and to gastric mucin without affecting the viability of either bacteria or gastric epithelial cells. Polysaccharides isolated from seaweed are preferred anti-adhesive materials and fucoidans is a most preferred embodiment. To facilitate bacteria eradication, methods include the administration of fucoidans before, during and/or after other killing and destroying physical or chemical therapy. The inhibition or impairment of the mechanism of bacterial adhesion due to the treatment with fucoidans is aimed to diminish colonization and pathogenesis of pathogenic bacteria by making them more fragile or susceptible to killing or destroying therapies. The combined use of fucoidans with PDT is a preferred method to eradicate H. Pylori in the gastrointestinal tract.
WO2013147577A1 Semi-solid topical composition which contains pirfenidone and modified diallyl disulphide oxide (m-ddo) for eliminating or preventing acne The present invention relates to a semi-solid topical composition which contains pirfenidone and an anti-microbial/antiseptic such as modified diallyl disulphide oxide (M-DDO) and to the method for manufacturing same, which has advantages over other pharmaceutical forms for cutaneous delivery known in the prior art, which can be used as an anti-fibrotic, anti-inflammatory and antiseptic agent in the prevention, treatment and reversal of acne and post-acne lesions. Said composition can also be used to reduce the redness of the skin, to halt the formation of new outbreaks of acne, to reverse existing outbreaks and to regenerate skin damaged by acne.
WO2006029863A1 Thiazolinone 2-substituted quinolines The present invention provides thiazoline substituted quinoline derivatives, where the quinoline ring is substituted at the 2 position, of formula (I) which derivatives demonstrate CDK1 antiproliferative activity and are therefore useful as anti-cancer agents, pharmaceutical compositions containing said compounds as well as processes for their manufacture.
CN101314043B Preparation method of podophyllinic acid lactone derivant The invention provides a derivative for podophyllotoxin. The derivative is characterized in that the derivative is a carboxyl single methoxypolyethylene glycol derivative of podophyllotoxin with the following structural formula. The preparation method comprises the following the steps that: the podophyllotoxin, the carboxyl single methoxypolyethylene glycol, dicyclohexyl imine and N dimethylaminopyridine are used as raw materials to prepare the polyethylene glycol derivative of the podophyllotoxin by the microwave catalytic action. The podophyllotoxin prodrug of the derivative is good in solubility and high in stability. The preparation of the derivative has the characteristics of high efficiency, rapidness, simpleness and convenience and high reaction yield.
EP2638038A1 Method of treatment for mental disorders The invention relates to a medicament or a method for treating mental disorders, in detail, ADHD comprising lurasidone, or a combination of lurasidone and a D4 receptor agonist.
EP1603894B1 Pharmacologically active novel dauer pheromone compound for controlling aging and stress and method for isolating and characterizing the same The present invention discloses a method for effectively isolating and purifying a physiological active dauer pheromone compound having the following structural formula I related to aging and stress of C. elegans, and determination of the structure of such material. First, ethanol extract is prepared by completely concentrating a liquid medium with ethanol after culturing C. elegans on a S. basal liquid medium, and then this ethanol fraction is further extracted with ethyl acetate. Then, impurities are removed from ethyl acetate extract by a silica-gel adsorption chromatography and a pheromone extract is isolated and purified by amine column chromatographic procedures using various solvents as eluent. Finally, a pheromone compound having structural formula I is completely isolated and characterized by size-exclusion HPLC.
EP2608783A1 Use of glycyrrhetinic acid, glycyrrhizic acid and related compounds for prevention and/or treatment of pulmonary fibrosis The present invention pertains to novel uses of glycyrrhetinic acid (GA), glycyrrhizic acid (GLA) and related compounds for prevention and/or treatment of pulmonary fibrosis, in particular, irradiation-induced pulmonary fibrosis. Also embodied are therapeutic uses of prodrugs, metabolites, derivatives (e.g., acids, esters and ethers), and salts of glycyrrhetinic acid (GA) and glycyrrhizic acid (GLA). The present invention also provides for therapeutic or pharmaceutical compositions comprising a compound of the invention in a form that can be combined with a pharmaceutically acceptable carrier.
US20120107250 Abuse-proofed dosage form An abuse-proofed, thermoformed dosage form containing, in addition to one or more active ingredients with abuse potential optionally together with physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N and to a process for the production thereof.
CN103656656A Sorafenib tosylate pharmaceutical composition and preparation method The invention discloses sorafenib tosylate pharmaceutical composition which is characterized by comprising the components in percentage as follows: 10%-50% of sorafenib tosylate, 20%-50% of lactose, 10%-30% of microcrystalline cellulose, 5%-10% of crospolyvinylpyrrolidone, 1%-5% of beta-cyclodextrin and 1%-2% of superfine silica powder. The sorafenib tosylate pharmaceutical composition is good in stability and has more remarkable advantages of product yield improvement, cost reduction, industrialization and better clinic application.
WO2008091195A1 Novel heteroaryl substituted imidazo [1,2 -a] pyridine derivatives The present invention relates to novel heteroaryl substituted imidazopyridine derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted imidazopyridine derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measureing clinical efficacy of Alzheimer's disease therapeutic agents.
CN101269003A Oral preparation containing roxithromycin, preparation method and application thereof The invention relates to a buccal preparation containing roxithromycin as well as a preparation method and usage thereof. The invention aims at providing a buccal preparation taking roxithromycin as ingredient, which is dissolved in saliva of oral cavity by sucking to enter the periphery of the oral cavity, the pharyngeal portion and the pharyngeal tonsils part, so as to play the role of antibacterium. The buccal preparation takes the roxithromycin and ramification thereof as the raw material, and can be made into preparations such as buccal tablet, candy and pill, etc. The buccal preparation has the characteristics of rapid effect, good healing efficacy and convenient administration, etc., and can directly increase the concentration of bacteriophage drug at the parts of pathological changes, enhances the antibacterial capacity and is more suitable for the patients.
CN101982467A Lignans compounds contained in Schisandra chinensis, and preparation method and application thereof The invention discloses lignans compounds contained in Schisandra chinensis, and a preparation method and an application thereof. The compounds have the structure of a novel general formula (I). The preparation method of the invention comprises the steps of grinding a Schisandra chinensis sample, performing ultrasonic extraction for 3 times by 95% ethanol, merging the extracting solutions and concentrating to form an extract, performing primary separation on the extract by silica gel column chromatography, and then further separating by the high performance liquid semi-preparative chromatography to obtain the novel compounds with the name of Yunnan-Tibet Schineglphenol A. The compounds are subjected to the antioxidative activity detection and the effect experiment for eliminating the freeradicals in the main stream smoke of the cigarette, and the experimental result indicates that the compounds have good antioxidative activity and good free radicals eliminating effect.
CN102485224A Method for preparing micronized oxazolidinone medicines and micronized pharmaceutical composition The invention provides a method for preparing micronized oxazolidinone medicines and a micronized pharmaceutical composition. The method comprises the following steps: (a) mixing solid oxazolidinone compounds with a solid micronization auxiliary agent according to a weight ratio of 100:20 to 100:0.5 so as to obtain a solid mixture; (b) carrying out micronization on the solid mixture obtained in step (a) so as to obtain medicine particles with a particle size D(90) of no more than 10 mu m. The invention also provides the pharmaceutical composition containing the medicine particles. The micronization method provided in the invention enables the phenomena of caking and obstruction in crushing to be greatly reduced and solubility, yield and crushing efficiency of the micronized medicines to be substantially improved; the pharmaceutical composition prepared in the invention can improve in vitro dissolubility and in vivo absorption of the medicines.
CN1823806A Ground erythromycin soft capsule and its preparation method A soft capsule of dirithromycin is prepared from dirithromycin and the excipients chosen from diluent, cosolvent, solubilizer, suspending aid and surfactant. Its preparing process is also disclosed.
WO2012112447A2 Histone deacetylase inhibitors and methods of use thereof The present invention provides novel compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of a compound of the invention to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
CN103420931A Pentacyclic compound capable of adjusting polarization of macrophages and resisting diabetes and application thereof The invention discloses a pentacyclic compound capable of adjusting polarization of macrophages and resisting diabetes, and application thereof. The pentacyclic compound JM-00121 has a molecular structure as shown in the description and can be used for curing type II diabetes and symptoms related to the diseases including adiposity, lipid disease, diabetes nephrosis, diabetes type dyslipidemia, hyperlipidemia, atherosclerosis, hepatic fibrosis and the like.
US7282500 Nitrogen compounds such as 4-(1-Hydroxyimino-indan-5-yl)-5-pyridin-4-yl-1H-imidazole-2-carboxylic Acid (2-morpholin-4-yl-ethyl)-amide, used as anticarcinogenic agents and for prophylaxis of brain disorders The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, use as Raf Kinase Inhibitors and treatment methods for neurotraumatic diseases and cancer.
CN1795850A Composition for preventing or curing SARS, and health food of containing the composition A composition for preventing and treating severe acute respiratory syndrome (SARS) features that it contains catechins. A health-care food containing said composition is also disclosed.
US20060058317 Oxazolidinone derivatives as antibacterial A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: formula (I), wherein C is selected from D and E, formula (D), formula (E), R2a, R6a, and R3a are independently selected from for example H, CF3, Me and Et; R2b and R6b are independently selected from for example H, F, CF3, Me and Et; R1b is —X-Z wherein X is O or S and Z is a C-linked 5- or 6-membered heteroaryl ring; R4 is for example an optionally substituted 5- or 6-membered heterocyclic ring system. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described.
US8258288 RNA interference mediated inhibition of respiratory syncytial virus (RSV) expression using short interfering nucleic acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating sespiratory syncytial virus (RSV) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of RSV gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of RSV genes, including cocktails of such small nucleic acid molecules and lipid nanoparticle formulations of such small nucleic acid molecules cocktails thereof. The application also relates to methods of treating diseases and conditions associated with RSV gene expression, such as RSV infection, respiratory failure, bronchiolitis and pneumonia, as well as providing dosing regimens and treatment protocols.
EP2079715A1 Triazines and their use as inhibitors of metalloproteinases The present invention relates to compounds or pharmaceutically acceptable salts thereof, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in therapeutical use. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and various physiological and pathophysiological processes.
WO2013082875A1 Arsenic compound solution and albumin nanoparticle and lyophilized preparation entrapping arsenic compound prepared using same An arsenic compound solution, and an albumin nanoparticle and a lyophilized preparation prepared using same and entrapping an arsenic compound. The arsenic compound solution is prepared using the following method: adding As2O3 powder in sterile deionized water to obtain a suspension, 6 to 25 mg of As2O3 powder being added in every mL of sterile deionized water; dripping an NaOH solution to the obtained suspension until the powder is fully dissolved and adjusting the pH of the solution to 7.5 to 9, and making the concentration of the obtained arsenic compound solution be 5 to 20 mg/mL in terms of the added As2O3. The albumin nanoparticle is prepared by mixing an albumin solution and the arsenic solution with the mass ratio of the added As2O3 in the arsenic compound solution to the albumin being 1: 5 to 20 and using a method of solvent removing and physical curing.
US20090075944 Deuterium-enriched ibandronate The present application describes deuterium-enriched ibandronate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN102924476A Novel oxazine compounds and application thereof The invention belongs to the technical field of medicines and relates to oxazine compounds and medical application thereof. The oxazine compounds and salts obtained by the addition of pharmaceutically applicable acids of the oxazine compounds are taken as platelet aggregation inhibitors. Structural general formulas of the oxazine compounds are shown in the specification. In the structural formula I, II, III, IV, V or VI, R can be independently selected from H, alkyl groups of one to four carbon atoms, benzyl, or a substituted or unsubstituted aromatic group. The synthetic method for the compounds is simple, and adapts to the industrialized production; compared with natural analogues, the compounds are relatively stable; and the biological activity assay displays that the compounds have the effects of easing pain, resisting inflammation and resisting procoagulant activity, and are a medicine for resisting platelet aggregation.
US20070259955 Process for the Preparation of Nateglinide A one-pot process for the preparation of nateglinide, which process comprises reacting an alkyl ester of D-phenylalanine of formula (II): where R represents C1-4alkyl, typically methyl, either as the free base or in salt form (typically the hydrochloride), with trans-4-isopropylcyclohexanecarboxylic acid of formula (III): where X represents hydroxy or halo, typically chloro, to obtain a C1-4 alkyl ester of nateglinide of formula (IV), preferably the methyl ester of nateglinide: followed by hydrolysis to yield nateglinide of formula (I):
US20060247451 Crystalline base of citalopram The present invention relates to the crystalline base of the well known antidepressant drug citalopram, 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of citalopram, such as the hydrobromide, using the base, the salts obtained by said process and formulations containing such salts.
US20050064407 Bcl-2 dnazymes The present invention provides DNAzymes which specifically cleaves mRNA transcribed from a member of the bcl-2 gene family selected from the group consisting of bcl-2, bcl-xl, bcl-w, bfl-1, brag-1, Mcl-1 and A1. The DNAzymes comprise (a) a catalytic domain that has the nucleotide sequence GGCTAGCTACAACGA (SEQ ID NO.1) and cleaves mRNA at any purine: pyrimidine cleavage site at which it is directed, (b) a binding domain contiguous with the 5′ end of the catalytic domain, and (c) another binding domain contiguous with the 3′ end of the catalytic domain. The binding domains are complementary to, and therefore hybridise with, the two regions immediately flanking the purine residue of the cleavage site within the bcl-2 gene family mRNA, at which DNAzyme-catalysed cleavage is desired. Each binding domain is at least six nucleotides in length, and both binding domains have a combined total length of at least 14 nucleotides.
EP2736514A1 Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
CN102757461A Modified lecithin complexed iodine, and preparation method and application thereof The invention relates to a modified lecithin complexed iodine, and a preparation method and application thereof. The modified lecithin complexed iodine has the structure disclosed as Formula (1), wherein R1 and R2 independently represent alkyl groups of saturated fatty acids. The modified lecithin complexed iodine has high stability; and like the lecithin complexed iodine, the modified lecithin complexed iodine can be used for treating bronchocele, hypothyroidism of children, and other adaptive diseases caused by iodine, can enhance the retina metabolism, and has the advantages of favorable dependence and definite curative effect. Compared with the lecithin complexed iodine, the emulsification stability and dispersity of the modified lecithin complexed iodine are improved, and the oxidation resistance is greatly enhanced, thereby being beneficial to the quality and stability of the medicines.
US20080200449 For treating pulmonary hypertension; device can provide patients with a high degree of autonomy Treprostinil can be administered using a metered dose inhaler. Such administration provides a greater degree of autonomy to patients. Also disclosed are kits that include a metered dose inhaler containing a pharmaceutical formulation containing treprostinil.
US20080161282 Cytotoxic agents and methods of use Disclosed are compounds that inhibit proteasomic activity in cells. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly cell proliferative conditions, such as cancer and inflammatory conditions.
CN102633794A 5-substituted phenoxy-1, 2, 4-triazole [4, 3-a] pyridine compound used for antiepileptic medicament, and medical salt thereof The invention relates to a 5-substituted phenoxy-1, 2, 4-triazole [4, 3-a] pyridine compound used for antiepileptic medicament, and medical salt of the compound. The invention provides the new 5-substituted phenoxy-1, 2, 4-triazole [4, 3-a] pyridine compound which has comparatively low toxic and side effects and shows the valuable pharmacological properties as anticonvulsant, and addition salt of pharmaceutically acceptable acid of the compound. The formula I shows the compound and the addition salt of the pharmaceutically acceptable acid of the compound, wherein R is selected from all bromoalkanes. The compound is high in anticonvulsion activity, comparatively low in toxic and side effects and high in safety index, thus laying the foundation for the research and application of the antiepileptic medicament.
US20090182013 Derivatives of 5-Thioxylopyranose and Use of Same for Treatment The invention relates to new compounds of 5-thioxilose, preferably derivatives of the 5-thioxilopyranose type, and to a method for preparing the same and their use as the active ingredient of drugs mainly intended for treating or inhibiting thrombosis or heart failure or thromboembolic diseases.
WO2014037327A1 N-cyclopropyl-n-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof The present invention relates to compounds of general formula (I), wherein R1, LP, LQ, (Het)Ar, m and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR1 19 receptor and modulate its activity.
US20130040959 Heterocyclic Quinolizine Derived M1 Receptor Positive Allosteric Modulators The present invention is directed to novel 3-oxo-2,3-dihydropyrazolo[4,3-c]quinolizine derived compounds of generic formula (I) or a pharmaceutically acceptable salt thereof, which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
CN103263398A Cefdinir composition capsule and preparation method thereof The invention relates to the field of pharmaceutical preparations and particularly discloses a cefdinir composition capsule and a preparation method thereof. Pharmaceutical effective ingredients of the cefdinir composition capsule disclosed by the invention comprise cefdinir, microcrystalline cellulose, potassium polacrilin, cross-linked sodium carboxymethyl cellulose, talcum powder, 95% ethanol, magnesium stearate, methyl-2-hydroxyethyl acrylate and succinic acid. According to the cefdinir composition capsule, cefdinir, microcrystalline cellulose, potassium polacrilin, cross-linked sodium carboxymethyl cellulose, talcum powder, 95% ethanol, magnesium stearate, methyl-2-hydroxyethyl acrylate and succinic acid preferably serve as the pharmaceutical effective ingredients of the cefdinir composition capsule, and the stability, fluidity and dissolution of cefdinir are improved through mutual synergism, so that the use safety and long-term storage of clinical drugs are facilitated.
US8039011 A temperature change composition including a neurosensory component, e.g., menthol, and a first phase change component having a first phase change temperature between 15-40 degrees C., e.g., hydrocarbon, wax; encapsulated evaporative cooling agent; refreshing; durability; receptivity with other skin item Provided is a temperature change composition including a neurosensory component; and a first phase change component having a first phase change temperature between about 15 degrees C. and about 40 degrees C. Also provided is a temperature change composition including an evaporative cooling component; and a first phase change component having a first phase change temperature. Also provided is a temperature change composition for cooling skin, the composition including a first phase change component having a first phase change temperature; and a second phase change component having a second phase change temperature different from the first phase change temperature.
CN101224205B Composition of atorvastatin and levorotatory amlodipine and preparing method thereof The invention relates to a combination of atorvastatin and levamlodipine, mainly consists of levamlodipine or officinal salt thereof, atorvastatin or officinal salt thereof, alkali metal salt, and cyclodextrin and derivatives thereof and guarantees the stability and the bioavailability of atorvastatin and levamlodipine.
CN102850403A Water-soluble iron carbonyl compound, and preparation method and application thereof The invention discloses a water-soluble iron carbonyl compound, and a preparation method and an application thereof. The compound has a structural formula represented by the formula (1). When the compound is subjected to a reaction with mercaptoethylamine, CO can be released. The compound provided by the invention has good water solubility and appropriate stability. Metal ions and organic ligands involved in the reaction have good biocompatibility. Residual substances after CO releasing are harmless or slightly toxic to bodies. The timing and rate of CO releasing are easy to control.
CN1985878A Medicine composition for treating peptic ulcer and its preparing method The present invention provides a kind of medicine composition for treating peptic ulcer and its preparation process. The medicine composition is prepared with licorice flavonid, copper sodium chlorophyll, cuttlebone and propantheline bromide. The medicine composition has excellent treating effect on the peptic ulcer caused by hyperactive liver qi attacking the stomach, moist heat stagnation, deficiency cold of spleen and stomach, stomach yin deficiency, and depressed liver with insufficient spleen.
WO2009100370A1 Methods of treating migraine based on rhythmic sodium levels The present invention provides precise timing of the administration of therapeutic agents for treating migraine and methods of treating migraine based on the cerebrospinal fluid ('CSF') sodium rhythms. Specifically, the present invention provides methods of treating migraine and methods of administering to an individual an effective amount of a therapeutic agent that relieves one or more symptoms of migraine by following a administration regime that is timed according to a sodium rhythm in the CSF that has been predetermined for a population of individuals.
US7323469 tyrosine kinase inhibitors; for the treatment especially of a proliferative disease, such as a tumor The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.
US20080227749 Dyspareunia; vaginal and/or vulvar administration of formulations as a lubricant A method is provided for treating a female individual who suffers from or is prone to dyspareunia. The method involves vaginal and/or vulvar administration of a formulation comprising a therapeutically effective amount of a carrageenan and a pharmaceutically acceptable aqueous carrier. In addition, a carrageenan-based formulation is provided as a new composition of matter. Packaged kits for an individual to use in the administration of a carrageenan-based formulation as provided as well.
CN102085228A Medicinal drop pills for treating menopause syndrome The invention discloses medicinal drop pills for treating menopause syndrome. The medicinal drop pills are prepared by the following steps of: extracting 55 parts of epimedium, 80 parts of glossy privet fruit, 1 part of vitamin B1, 1.5 parts of oryzanol and 1 part of vitamin B6 serving as raw materials, adding polyethylene glycol 4000, mixing uniformly and dropping. The medicinal drop pills have the effects of warming the kidney and nourishing yin, adjusting and replenishing yin and yang and treating the menopause syndrome, and have the characteristics of quick effect, exact efficacy, high safety, small dose and the like.
US6838468 4-(phenyl-piperdin-4-ylidene methyl)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders Compounds of general formula I[Chemical formula should be inserted here. Please see paper copy] R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1,2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.
WO2014014363A1 Injectable antibiotic formulations and their methods of use This invention relates to a composition, including penethamate (PNT ) or a pharmaceutical equivalent thereof; and at least one oily vehicle.
CN102361872A Fused pyrimidines as AKT inhibitors The present invention relates to compounds of formula (I), a N-oxide or tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6, R7, R10, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
WO2014015054A1 Beta amino acid derivatives as integrin antagonists Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.
WO2008076045A1 Novel 2-amino- 5-aryl-imidazol-4 -ones This invention relates to novel compounds having the structural formula (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
WO2008073956A2 Cyclic sulfonamide derivatives and methods of their use The present invention is directed to cyclic sulfonamide derivatives of formula (I): or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behaviorial disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.
WO2005102393A1 Patch for external use with elevated content of absorption promoter in pressure-sensitive adhesive base A pressure-sensitive adhesive composition for transdermal absorption which contains a drug and a transdermal absorption promoter for the drug, characterized by further containing polyvinylpyrrolidone so as to stabilize the transdermal absorption promoter contained in the adhesive composition. Thus, the transdermal absorption promoter can be prevented from vaporization or degradation and a patch for external use containing the transdermal absorption promoter at a high concentration in using can be provided.
US20080280878 Blocking HSP90, particularly ansamycin or 17-allylamino-17-demethoxygeldanamcin; controlling gene expression; tyrosine lkinase inhibitor Novel method of treating chronic lymphocytic leukemia by the administering of HSP90 inhibitors, particularly ansamycins, more particularly I 7-allylamino-I 7-demethoxygetdanarnycin (17-AAG).
WO2011127833A1 Benzoheterocyclic compounds, preparation methods and uses thereof A kind of non-nucleoside antiviral inhibitors, more especially, benzoheterocyclic compounds shown as general formula I or their pharmaceutically acceptable salts or hydrates and preparation methods thereof are provided. These compounds or their pharmaceutically acceptable salts or hydrates can inhibit hepatitis B virus (HBV) DNA replication and hepatitis C virus (HCV) RNA replication, and can be used in the manufacture of medicaments for preventing and/or treating viral infections, especially HBV infections and HCV infections.
CN102311389A Azoaryl substituted pyrazole derivative and synthesis as well as anti-cancer application thereof The invention provides a compound (I) or (II) and a salt thereof. The compound has an excellent suppression effect on tumor. The invention also provides a synthesis process for the compound (I) or (II) and an intermediate thereof.
US20120288531 pharmaceutical compositions for delivery of ferric iron compounds, and methods of use thereof The pharmaceutical compositions described comprise a therapeutically effective amount of a ferric compound and at least one bioavailability enhancer for oral delivery. Some pharmaceutical compositions described herein include a suspension which comprises an admixture in solid form of a therapeutically effective amount of a ferric compound and at least one bioavailability enhancer (e.g. a salt of a medium chain fatty acid) and a lipophilic medium. The pharmaceutical compositions may be enteric-coated. Methods of treating or preventing diseases by administering such compositions to affected subjects are also disclosed. The methods of treatment described herein increase the level of iron in the bloodstream of a subject by administering to the subject an effective amount of an oral composition of a ferric iron compound.
US20090221691 Compositions and methods for inhibiting g protein signaling The present invention relates to methods for identifying agents which bind to specific amino acid residues of the protein interaction site of G protein β protein subunit. Compounds identified in accordance with the assay of the invention and methods for using the compound for modulating at least one activity of a G protein are also provide.
US7141599 Immunosuppressive effects of administration of a cyclooxygenase-2 inhibitor, a leukotriene B4 receptor inhibitor and a cyclosporin Treatment with a cyclooxygenase-2 inhibitor and a leukotriene B4 receptor antagonist is described as being useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune diseases.
WO2012054738A1 Combination of an aminoacyl - trna synthetase inhibitor with a further antibacterial agent for attenuating multiple drug resistance Bacterial multidrug resistance is attenuated in a subject by administering an aminoacyl-tRNA synthetase inhibitor and an antibacterial agent to the subject, wherein the aminoacyl-tRNA synthetase inhibitor is distinct from the antibacterial agent.
US20100316594 Modified 2' and 3' nucleoside prodrugs for treating flaviviridae infections 2′ and/or 3′ prodrugs of 1′, 2′, 3′ or 4′-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.
EP2626352A1 Heterocyclic low-molecular sapp mimetics, a pharmaceutical composition and methods for producing and using same The invention relates to a novel class of non-peptide heterocyclic low-molecular peptide mimetics of secretory amyloid precursor protein (sAPP mimetics) capable of acting effectively upon the processes of the formation, storage and regeneration of normal and pathological memory. The compounds can also be used for studying (in vitro and in vivo) biochemical signaling, neurotrophic and neuroprotective processes related to the secretory protein sAPP and for studying the mechanisms of the formation, storage and regeneration of memory. Specifically, the invention relates to (azaheterocyclyl)alkyl derivative amides of 2-(het)arylglycines of general formula (I) in which: n and m can have the values 0, 1, 2 and 3; the symbol (#) here and hereinafter signifies the possible presence of a chiral centre; R represents optionally substituted C5-C10aryl or a 5-7-membered hetaryl containing 1-3 heteroatoms selected from nitrogen, oxygen and sulphur and optionally condensed with a benzene ring; A1 and A2 independently represent an optionally substituted, 3-7-membered, saturated, partially saturated or aromatic azaheterocycle which contains from 1 to 3 atoms of nitrogen in the cycle and is optionally condensed with a benzene ring; or their pharmaceutically acceptable salts or alkyl esters in the form of individual optical isomers, or combinations thereof.
EP1329504B1 Nucleic acid of novel human kinesin-associated gene, protein encoded by the nucleic acid, peptide fragment thereof and anticancer agents comprising the nucleic acid and the like Base sequence data of a human kinesin-associated gene having a motor domain; and data of the functions of a protein encoded by the above-described human kinesnin-associated gene and another protein encoded by a human kinesin-associated gene having no motor domain. These data are applied to diagnosis (for example, judgment of the prognosis of neuroblastoma) and treatment for, in particular, malignant tumor as antisense nucleic acids.
US20120277173 Stabilized anthocyanin compositions The invention describes stabile anthocyanin compositions, methods to prepare such compositions and also methods of use of such compositions to treat various afflictions. The present invention describes unique compositions of an anthocyanin and a stabilizing compound such that the combination of the two components provides that the anthocyanin does not readily undergo degradation, such as oxidation, pH instability, etc.
CN101497600A 2,4,5- tri-substituted-1,3-dithiolane, synthesizing method and use thereof The invention discloses 2,4,5-trisubstitution-1,3-dithiolane, a method for synthesizing the same and application thereof. The preparation method comprises: 1, preparing 2-(2,2-dimethoxyethyl)-4,5-bis methoxycarbonyl-1,3-dithiolane; 2, reducing the 2-(2,2-dimethoxyethyl)-4,5-bis methoxycarbonyl-1,3-dithiolane to 2-(2,2- dimethoxyethyl)-4,5-dihydroxyl-1,3-dithiolane; and 3, coupling Boc-L-amino acid with the 2-(2,2-dimethoxyethyl)-4,5-dihydroxyl-1,3-dithiolane to generate the 2-(2,2-dimethoxyethyl)-4,5-di-(N-Boc-L-amino acyloxy methyl)-1,3- dithiolane, and removing protecting groups. In vitro and in vivo test results show that the compound has excellent activity in inhibiting proliferation of tumor cells, and can be clinically used as an anti-tumor agent.
CA2606042A1 Stop-and-go oxaliplatin treatment regimens Methods of treating an oxaliplatin-sensitive cancer are disclosed in which a therapy comprising oxaliplatin is initiated, continued until a predetermined endpoint, stopped, then reintroduced after specific criteria are met. This stop-and-go approach reduces or eliminates the neurotoxicity associated with oxaliplatin administration while at the same increasing one or more of the beneficial effects of oxaliplatin therapy.
CN103040823A Application of vinpocetine in preparation of anti-angiogenic medicament The invention relates to application of vinpocetine in preparation of an anti-angiogenic medicament. So far, reports on an anti-angiogenic activity of the vinpocetine are not seen. The invention provides application of the vinpocetine in preparation of the anti-angiogenic medicament, antineoplastic medicament and exudative senile macular degeneration medicament. An in vivo pharmacodynamic experiment carried out by a zebra fish angiogenesis model confirms that the vinpocetine can inhibit the zebra fish angiogenesis remarkably and the growth of the transplanted human cancer cells, and has a treatment effect on exudative senile macular degeneration. Thus, the vinpocetine can be applied to the preparation of the anti-angiogenic medicament, the antineoplastic medicament and the exudative senile macular degeneration medicament.
CN1861065A Formula and prepn. method for compound ointment contg. zinc undecenate A composite zinc undecylenate ointment is prepared from andecin, zinc oxide, glycerin, CMC-Na, water, and sodium laurylsulfate through reaction to obtain zinc undecylenate, dispersing and diluting.
CN1985826A Injection containing tricyclofluoro quinolone sulfonate and its preparing method and use The present invention provides one kind of injection containing (+/-) 6-fluoro-1-methyl-7(1-piperazine)-4-oxo-4H-[1, 3] thioazetidine (3, 2-a) quinolyl-3-carboxylic mesylate and its preparation process. The injection may be prepared into freeze dried powder for injection and injection liquid. The present invention overcomes the difficult of industrially preparing and clinically applying (+/-) 6-fluoro-1-methyl-7(1-piperazine)-4-oxo-4H-[1, 3] thioazetidine (3, 2-a) quinolyl-3-carboxylic acid.
CN102100693A Artificial tears including carnosine and preparation method thereof The invention relates to artificial tears, in particular to artificial tears including carnosine, concretely, the artificial tears including carnosine comprise the following components and contents in percentage by weight: 0.2-5.0 percent of carnosine, an osmotic pressure regulator, a pH regulator and the balance of water, wherein the osmotic pressure regulator makes the mill-osmotic pressure mol concentration ratio of the artificial tears be between 0.9 and 1.1, and the pH regulator makes the pH value of the artificial tears be between 5.0 and 9.0. The artificial tears including carnosine can be used for treating dry eye syndrome, and also has a function of preventing cataract. The invention also relates to a preparation method of the artificial tears.
WO2010054024A3 1, 2 -thiazol yl derivatives as cannabinoid receptor ligands The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.
EP1618883A1 Agent for preventing and ameliorating constipation A novel agent for preventing and healing constipation which heals the symptom of constipation very effectively and entails absolutely no side effect is provided. This agent for preventing and healing constipation is formed by containing a hydrogen of a polyvalent metal salt of alginic acid possessing a spherical or ovaloid shape having a short diameter in the range of 1 - 10 mm and an aspect ratio (long diemter/short diameter) in the range of 1 - 25. The hydrogel of a polyvalent metal salt of alginic acid is obtained by dropping an aqueous solution of sodium alginate into an aqueous solution of a polyvlant metal salt. It is optionally stored in water and/or a hydrogen compound of a natural compound possessing a free acid group capable of reacting and sequestering a basic compound.
US20130045960 Abuse-Deterrent Pharmaceutical Compositions of Opiods and Other Drugs An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.
CN101422442A Levetiracetam osmotic pump controlled release tablet and preparation method thereof The invention belongs to the technical field of medicament and provides a Levetiracetam osmotic pump controlled-release tablet and a preparation method thereof. The invention consists of the accessory of the Levetiracetam playing the effect of release control and a semi-transparent membrane; in the invention, proper accessory and medicament are mixed to press a tablet core at first; then a layer of semi-transparent membrane is coated outside the tablet core; then at least one small hole is punched on the semi-transparent membrane so as to lead active matters to be released from the semi-transparent membrane, thereby controlling the release of the medicament. Compared with a common preparation, the controlled-release preparation prepared by the invention has the advantages of small wave range of the blood medicine concentration, reducing toxic and side effect, being taken once in one day and improving the compliance of sufferers. The controlled-release preparation is applied on the adjunctive therapy for the partial seizure of epileptics in clinic.
WO2014118135A1 Amidoimidazopyridazines as mknk-1 kinase inhibitors The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I) : in which A, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
US20130023526 Isoxazolines as Therapeutic Agents The present invention provides compound of Formula (I) biologically active metabolites, pro-drugs, isomers, stereoisomers, solvates, hydrates and pharmaceutically acceptable salts thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological conditions.
CN103086862A Hydroxydecyl quinone derivative for treating or preventing nerve diseases The invention relates to a hydroxydecyl quinone derivative for treating or preventing nerve diseases. Specifically, the invention relates to the hydroxydecyl quinone derivative as shown in formula I, a pharmaceutical composition containing the compound as shown in the formula I, and a preparation method and uses of the hydroxydecyl quinone derivative in preparation of medicaments for cerebrovascular diseases. The compound disclosed by the invention can effectively treat or prevent the diseases or disease symptoms: the cerebrovascular diseases, improve cerebral metabolism and improve mental symptoms, activate brain mitochondrial respiratory activity, improve cerebral energy metabolism of cerebral ischemia, improve the utilization rate of cerebral glucose, increase the production of cerebral triphosadenine, inhibit the generation of lipid hydroperoxide from brain mitochondria and inhibit the membrane disorder caused by overoxidation action of the brain mitochondrial membrane lipid, reduce impaired brain functions caused by chronic cerebrovascular diseases, cerebral trauma and the like, improve subjective symptoms, language, anxiety, depression, hypomnesia, intelligence decrease and other mental and behavioral disorders, promote the intelligence, and activate brain mitochondrial functions, improve the cerebral energy metabolism and improve brain functions.
WO2012106702A3 Treatment of leukemia Compositions and methods for the treatment of leukemia by inhibiting FOXO signaling are described.
US20050234088 Urea substituted imidazoquinoline ethers Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and urea functionality at the I-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
CN101940581A Targeted medicinal composition for treating tumors The invention belongs to the field of biological medicaments, and relates to a targeted medicament for treating tumors in biomedicine, in particular to a targeted medicinal composition for treating tumors. The targeted medicinal composition comprises low-dosage mithramycin MIT and betulic acid BA medicaments; when the targeted medicinal composition is tested on tumor bearing nude mouse models of liver cancer, stomach cancer and cancer of pancreas, the influence on the generation of tumor vessels and the regulation of generated cell factors is observed, the results show that in a lower safe dosage range, the MIT alone cannot influence normal physiological activities of the test animals and inhibit the generation and growth of liver tumor vessels or can only cause little influence; but the medicinal composition of the invention can inhibit the generation of tumor vessels and further inhibit the growth of liver tumors without increasing the toxicity of medicaments.
US20120165342 Methods of Reducing Risk of Infection from Pathogens Prophylactic treatment methods are provided for protection of individuals and/or populations against infection from airborne pathogens. In particular, prophylactic treatment methods are provided comprising administering a sodium channel blocker or pharmaceutically acceptable salts thereof to one or more members of a population at risk of exposure to or already exposed to one or more airborne pathogens, either from natural sources or from intentional release of pathogens into the environment.
US7153959 treatment of tumor necrosis factor mediated disorders; asthma; inflammatory bowel disease; arthritis A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
CN103130790A 3-benzo isoxazole-4-benzpyrole maleimide derivative and application thereof The invention provides a 3-benzo isoxazole-4-benzpyrole maleimide derivative with a novel structure. The compound has efficient selective GSK (glaxosmithkline)-3beta inhibiting activity, and can be used for treatment of GSK-3beta mediate diseases such as diabetes mellitus, bipolar mental disorder, alzheimer disease, cancer, inflammatory disease, depressive disorder, neuroprotection and schizophrenia. The derivative is reasonable in design and simple and practical in preparation method. The structural general formula of the derivative is as shown in the specification.
WO2007062043A1 Method of activating murine toll-like receptor 8 The present invention provides a method of activation murine TLR8. Generally, the method includes contacting a cell expressing the murine TLR8 with a first IRM compound that comprises a TLR8 agonist, and contacting the cell expressing the murine TLR8 with a second IRM compound, wherein the second IRM compound comprises an oligonucleotide sequence comprising at least seven bases in length wherein at least one base is a thymine or a uracil.
CN1813739A Nalmefene hydro chloride lyophilized powder formulation for injection The present invention relates to a nalmefene hydrochloride freeze-dried powder injection preparation for injection. Said preparation is formed from effective component malmefene hydrochloride and proper medicinal carrier, in which the content range of nalmefene hydrochloride in the preparation is 0.1-4.5 mg generally, the medicinal carrier can be one or several kinds selected from mannitol, glucose, sodium chloride, beta-cyclodextrin, glucosan, fructose and sorbitol. The content range of said medicinal carrier can be 10-100 mg. the pH value of said preparation is 5.0-7.0.
WO2007068007A1 Use of a disinfectant for treating respiratory tract infections The invention provides method of administering a treatment to a patient infected with an infective agent, said method comprising forming inhalable particles of a disinfectant, inhaling the disinfectant particles to deposit the disinfectant on the infected surfaces of the respiratory tract, sinuses, and the lungs, and repeating the inhalation periodically until the level of infection has decreased. The invention further provides a single use container for use in the method and the use of a disinfectant in the preparation of a medicament.
US20100298341 Glycine Transporter-1 Inhibitors The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
WO2007007971A1 Pharmaceutical compositions comprising sibutramine The present invention provides a pharmaceutical composition for oral administration comprising: sibutramine in a free base form; an acidifying agent selected from the group consisting of citric acid, succinic acid, malic acid, maleic acid, and a mixture thereof; and a surfactant. Further, the present invention provides a pharmaceutical composition with improved stability comprising a sibutramine salt and an alkaline earth metal-free pharmaceutically acceptable additive.
US20050148627 Benzopyran compounds for use in the treatment and prevention of inflammation related conditions The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula 1 Wherein Z, X, R1, R2, R3, and R4 are as described in the specification.
CN102091147A Pharmaceutical composition for treating cognitive impairment and preparation method and applications thereof The invention belongs to the technical field of pharmacy, and in particular provides a pharmaceutical composition which is mainly composed of pseudo-ginseng and cape jasmine as crude medicines. The invention also provides a preparation method and applications of the pharmaceutical composition. Proved by experiments, the pharmaceutical composition provided by the invention has the efficacies of promoting blood circulation, removing obstruction in channels, detoxifying and promoting mentality, can effectively improve the cognitive function of patients with dementia or cognitive impairment, improves the abnormal behavior and life quality of patients, also can effectively target oxidative stress injury and micro-inflammation injury of brain cells, can increase energy supply for the brain cells, resists nerve cell apoptosis, promotes synaptic remodeling, has the effects of treating cognitive impairment, and is especially used for treating senile dementia or vascular dementia or minimal cognitive impairment or amnesia.
WO2013039880A1 Biomarkers and therapeutic targets of hepatocellular cancer Disclosed is a biomarker of Hepatocellular cancer (HCC), in particular stem cell like HpSC HCC subtype, and methods of using the biomarker, including methods for treating or preventing the cancer, diagnosis of cancer, methods of determining predisposition to cancer, methods of monitoring progression/regression of cancer, methods of assessing efficacy of compositions for treating cancer, as well as other methods based on the use of this cancer biomarker.
US20120321570 System for caries management by risk assessment The invention provides the tools needed for a dental patient's caries risk assessment. Included is a complete turnkey system for caries risk assessment and treatment, including an ATP test and a plurality of rinses and educational and diagnostic materials. The system for the detection and treatment of the bacterial infection that causes dental caries in a patient comprises a disposable ATP Bioluminescence sampler to swab areas of the patient's mouth, a bioluminescent light meter which measures the amount of ATP present in the patient's mouth, a rapid culture test for the detection of Mutans streptococci and lactobacilli, a diagnostic testing component that includes a caries risk assessment questionnaire, a treatment component that includes a short term therapeutic oral rinse of at least two components, and a long term maintenance rinse.
CA2268825C Immunostimulatory polynucleotide/immunomodulatory molecule conjugates Immunostimulatory polynucleotide-immunomodulatory molecule conjugate compositions are disclosed. These compositions include a polynucleotide that is linked to an immunomodulatory molecule, which molecule comprises an antigen and may further comprise immunomodulators such as cytokines and adjuvants. The polynucleotide portion of the conjugate includes at least one immunostimulatory oligonucleotide nucleotide sequence (ISS). Methods of modulating an immune response upon administration of the polynucleotide-immunomodulatory conjugate preparation to a vertebrate host are also disclosed.
WO2006112331A1 Novel condensed pyrrole derivative As a compound exhibiting a high DPP-IV inhibiting activity or improved in safety, toxicity, etc., there are provided compounds, or their prodrugs, or pharmacologically acceptable salts thereof, which compounds are represented by the formula: (I) wherein R1 is a hydrogen atom, an optionally substituted alkyl, etc.; R2 is a hydrogen atom, an optionally substituted alkyl, etc.; R3 is a hydrogen atom, a halogen atom, etc.; R4 is a hydrogen atom, a halogen atom, etc.; R5 is a hydrogen atom, a halogen atom, etc.; and Y is, for example, a group of the formula: (A) wherein ml is 0, 1, 2 or 3; and with respect to R6, either is none absent, or one or two thereof are present and each independently represent a halogen atom, etc.
EP2583965A1 Heterocyclic ring compound The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.
WO2009012223A1 Compositions for the treatment of metabolic disorders Preferred embodiments of the present invention are related to novel therapeutic drugs and drug combinations, and associated methods, for treating and/or preventing complications or otherwise treating disease in patients with hypertension, diabetes, metabolic syndrome, obesity and/or other metabolic disorders.
CN102846662A Oral body fluid replenisher The invention provides an oral body fluid replenisher. The oral body fluid replenisher comprises, in weight ratio, 5000-9000 milligrams of sodium chloride, 100-500 milligrams of potassium chloride, 50-500 milligrams of calcium citrate, 50-500 milligrams of calcium hydrophosphate, 10-50 milligrams of zinc sulfate, 5-50 milligrams of copper sulfate, 10-100 milligrams of ferrous sulfate, 5-500 grams of glucose and 1000 grams of purified water. A method for preparing the oral body fluid replenisher comprises the following steps of weighting raw materials according to the formula weight ratio; adding the raw materials in the purified water; and dissolving, stirring uniformly, standing for 2 hours, taking supernate, and bottling and packaging after being sampled, checked and qualified. Each bottle is filled with 200-500 grams of the oral body fluid replenisher, and the oral body fluid replenisher is sterilized at a high temperature and under high pressure or is degermed by ultra-filtration or is sterilized by cobalt CO60 and ultraviolet rays, and is cased to form finished products after being sampled, checked and qualified.
CN1759830A Enteric coated table of duloxetine, and preparation method A coated enteric tablet of Duluoxiding and its preparing process are disclosed. It features that said Duluoxiding can be released only in small intestine, so resulting in high biologic utilization rate.
CA2654315C Substituted 4-aryl-1,4-dihydro-1,6-naphthyridines and their use The present application relates to substituted 4-aryl-1,4-dihydro-1,6-naphthyridines of the formula (I):(see formula I) wherein Ar, R1, R2, R3 and R4 are as defined herein, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
CN101768202A Preparing method of high purity sarsasapogenin in rhizoma anemarrhenae and derivatives thereof, and medical new application thereof The present invention belongs to the technical field of medicine, which relates to a preparing method of high purity sarsasapogenin in rhizoma anemarrhenae and derivatives thereof, and medical new application thereof. Rhizoma anemarrhenae is extracted by ethanol containing water and/or water, the purity of the high purity sarsasapogenin prepared by the steps of adsorption elution by using macroporous absorbent resin, acid hydrolysis and recrystallization is up to 98%. Compared with the known art, the present invention has the advantages of low cost, low product impurity content and stable preparing art; the present invention is easy to operate and realize; and the production process has no pollution for the environment. A series of sarsasapogenin derivatives is also synthesized by a chemical synthesis method, and has anti-ageing activity by the certification of pharmacodynamics experiment. The new application of sarsasapogenin and the derivatives thereof in the preparation of senile dementia resistant drugs, anti-ageing drugs and antineoplastic is developed by the pharmacodynamics activity.
US20090263377 Il-32b-targeted diagnosis and therapy Methods for the diagnosis and treatment of IL-32β over-expressing cancers are provided. Also provided are methods for the treatment of wounds, hair loss and the promoting and/or restoration of hair growth utilized IL-32β antagonists. Finally, a sepsis model utilizing IL-32β is provided, as are methods for treating sepsis and inflammation using IL-32β antagonists.
US20120207850 Methods for Increasing the Kinetic Activity of Alcohol, Water and Other Liquids, so as to Render the Liquids More Useful in Enhancing the Alternative Cellular Energy Pathway in the Prevention and Therapy of Diseases The kinetic energy of liquids can be increased by several methods described in the present application. The methods include exposure to a magnetic field provided by a rotating or vibrating magnet; exposure to an electromagnetic field provided by an electrical power cord; and placement of the liquid within the vicinity of electrostatic energy and/or sound energy. A previously described method is the bubbling of electrolysis-generated water gas (Brown's Gas) into the liquid. The increased kinetic energy can be demonstrated using a previously described neutral red dye kinetic assay (NR-Kinetic assay). Energized liquids include alcohol, alcoholic beverages and water. The use of the energized solutions to enhance the alternative cellular energy (ACE) pathway in the therapy of individuals is described.
WO2007007132A1 Aripiprazole salts The present invention provides for new salts of aripiprazole of the general formula (II) formed with dibasic organic acids, camphorsulfonic acid, phosphoric acid, and processes for their preparation. Further objects of the present invention are pharmaceutical compositions containing said new aripiprazole salts. Aripiprazole salts according to present invention can be prepared by the reaction of aripiprazole base and suitable acid compounds in a molar ratio 0.5-3 based on the molar amount of aripiprazole in a suitable organic solvent.
EP1177177B1 Substituted 4-oxo-quinoline-3-carboxamides: gaba brain receptor ligands Disclosed are compounds of Formula (I) or the pharmaceutically acceptable salts thereof where, R1, R2, and W are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
WO2008109599A1 Pyrimido [5,4-c] quinoline-2, 4-diamine derivatives and methods of use thereof The present invention relates to Pyrimxdo [5,4-c]quinoline-2, 4 -diamine Derivatives, compositions comprising an effective amount of a Pyrimido [5, 4 -c] quinoline-2, 4 -diamine Derivative of formula (I), methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of an Pyrimido [ 5, 4 - c] quinoline-2, 4 -diamine Derivative. Disclosed are also methods for modulating PDK-I activity, comprising administering to a subject in need thereof an effective amount of a Pyrimido [5,4- c] quinoline- 2,4-diamine Derivative. The invention also relates to a process for preparing a Pyrimido [5,4- c] quinoline-2, 4 -diamine Derivative or a pharmaceutically acceptable salt thereof,
CN101797231A Method for controlling quality of Ceftezole sodium used for injection The invention discloses a method for controlling the quality of Ceftezole sodium used for injection, comprising the steps as follows: (1) controlling the moisture content of a Ceftezole sodium raw material to be 2-4%; and (2) controlling the humidity of the encapsulation environment to be 40-45%. By controlling the raw material moisture and the humidity of the encapsulation environment in the invention, the moisture content of a drug preparation can be controlled better so as to obtain a preparation with the characteristics of good clarity, favorable powder mobility and more accurate charging amount, thus being more applicable to clinic use.
WO2010099445A2 Non-covalent inhibition of the 26s proteasome and uses thereof The present inventions relate to compositions and methods for treating inflammatory diseases and cancer by administering proteasome inhibitors. In particular, the present inventions provide a new class of orally available non-covalent proteasome inhibitors capable of reducing NF-kappaB for mediating cytokine production in vivo. Further, the use of a small molecular weight inhibitor of the 26S proteasome via a non-covalent type inhibition is contemplated for use as a means to treat NF -kB mediated diseases, including but not limited to multiple myeloma and rheumatoid arthritis.
CN102846600A Oxiracetam drug activity composition and preparation method thereof The present invention provides an oxiracetam drug activity composition, which comprises the following components: a component I, a component II and a component III, wherein the component I is oxiracetam, the component I content is more than or equal to 98.0%, the component II is glycine anhydride, the component II content is more than 0 and is less than or equal to 0.3%, the component III is one or a plurality materials selected from 4-hydroxy-2-oxo-1-pyrrolidineacetic acid, 4-hydroxy-2-oxo-1-pyrrolidine, ethyl 4-hydroxy-2-oxopyrrolidine-1-acetate, methyl 4-hydroxy-2-oxopyrrolidine-1-acetate, and piracetam, the component III content is more than 0 and is less than or equal to 1.5%, the 4-hydroxy-2-oxo-1-pyrrolidineacetic acid content is more than 0 and is less than or equal to 0.5%, and the total content of the component II and the component III is less than or equal to 1.5%. The drug activity composition of the present invention has stable quality, and can completely meet quality requirements on the drug activity composition by oxiracetam preparations. In addition, the prepared preparation has characteristics of safety, effectiveness, and controllable quality, and clinical therapy effects and medication safety of the oxiracetam preparation are ensured.
US20110189175 Chronic lymphocytic leukemia prognosis and treatment Provided herein are methods for identifying a subject afflicted with chronic lymphocytic leukemia who is responsive to treatment with a chemotherapeutic agent by detecting the presence or absence of at least one APOE4 allele in the subject, the presence of an APOE4 allele identifying the subject as responsive to the treatment. Also provided are methods of treating a subject afflicted with chronic lymphocytic leukemia, including administering an estrogenic agent, an androgen withdrawal agent, an apoE4 peptide or mimetic thereof, and/or a chemotherapeutic agent in an amount effective to treat said chronic lymphocytic leukemia. Methods of determining a prognosis for a patient diagnosed with chronic lymphocytic leukemia are also provided. In addition, methods for stratifying a subject into a subgroup of a clinical trial and methods for identifying a patient in a clinical trial of a treatment for chronic lymphocytic leukemia are herein provided.
US20110281947 Methods of administering diclofenac compositions for treating photodamaged skin A method of treating at least one dermatological disorder selected from the group consisting of photodamage-induced wrinkles, rosacea, and acne, includes: (a) providing a composition containing 1-3 wt. % diclofenac or a salt thereof, 0.5-1.5 wt. % benzyl alcohol; 10-30 wt. % PEG monomethyl ether, 0.1-3.0 wt. % sodium hyaluronate; and 70-80 wt. % water; and (b) applying the composition to skin of a person in need of the treating in an amount effective to treat the at least one dermatological disorder.
US20120238509 Urocortin 2 analogs and uses thereof Disclosed are polypeptides that are analogs of urocortin 2 that have pharmacological activity similar to urocortin 2 but have improved water solubility compared to urocortin 2, and pharmaceutical compositions of the polypeptides of the present invention. Also disclosed are polynucleotides encoding the polypeptides, and methods of treating pathophysiological states employing pharmaceutical compositions of the polypeptides and polynucleotides of the present invention. In addition, disclosed are vectors and host cells that include a nucleic acid encoding a polypeptide of the present invention, and kits that include pharmaceutical compositions of the present invention.
CN102106849A Novel medicinal application of baicalein The invention discloses novel medicinal application of baicalein, in particular to application of the baicalein to the preparation of medicament for treating demyelinative diseases of central nervous system. The baicalein shows favorable treatment functions on an experimental allergic cerebrospinal meningitis model of a mouse and the treatment functions are achieved by inhibiting microglia 12/15 lipoxygenase in the central nervous system and adjusting the expression condition of a group of molecules with nerve protecting functions, such as FIZZ1 (foundininflammatoryzone1), MRC1 (mannose receptor, C type 1) and Arg1 (arginase 1) on the mRNA (messenger ribonucleic acid) level, thereby inducing high-level M2 type microglia in the central nervous system. The M2 type microglia has the function of CNS (central nervous system) neuroendocrine nutrilit and can promote the repair of medullary sheath, thereby relieving the progress of disease conditions.
CN101991555A Quetiapine fumarate tablet and preparation method thereof The invention relates to a quetiapine fumarate tablet and a preparation method thereof. The tablet of the invention comprises quetiapine fumarate, a filler, a disintegrant, povidone and magnesium stearate in certain proportions. The preparation method comprises the following steps: granulating the quetiapine fumarate, the filler and the disintegrant by a wet method; then adding the povidone and granulating into a soft material; screening, drying and finishing the soft material; adding the magnesium stearate and mixing; measuring the content and calculating the tablet weight; and respectively tabletting and coating to obtain the quetiapine fumarate tablet. The tablet can be used for treating schizophrenia. By using the formula provided by the invention, the defect of poor particle mobility during granulating in the prior art is overcome.
CN101703492A Tetrahydropalmatine transdermal patch and preparation method thereof The invention discloses a tetrahydropalmatine transdermal patch and a preparation method thereof. The patch comprises a back lining layer, a drug-storage layer and a protective layer, wherein the raw materials of the drug-storage layer comprise tetrahydropalmatine and pressure sensitive adhesive, or a moderate amount of transdermal accelerant and the like is added to finally prepare the tetrahydropalmatine patch. The tetrahydropalmatine patch has the advantages that the patch has convenient use, high bioavailability and lasting action and avoids liver 'first pass effect' and damages on gastrointestinal tract; and the patch reduces drug toxicity and side effects and increases drug bioavailability and therapeutic safety, thereby having outstanding anti-inflammatory and analgesic effects.
CN101984963A Application of T-2 toxin to preparing drugs for treating pancreatic carcinoma The invention discloses new application of T-2 toxin, namely application of T-2 toxin to preparing drugs for treating pancreatic carcinomas. The effective treatment amount of T-2 toxin is 0.1-20mg/Kg, preferably 0.5-8mg/Kg. The drugs are administrated by implantation, oral administration, intravenous injection, hypodermic injection and intramuscular injection, preferably intra-tumor injection. The inventor builds various solid tumor models and then examines the inhibiting effect of T-2 toxin on the tumors or tumor cells by carrying out intra-tumor injection or culture with cells on T-2 toxin.Experiments show that intra-tumor injection has confirmed curative effect on the tumors, especially the solid tumors hard to excised and drug administration through intra-tumor injection can further reduce the side effect range and degree of T-2 toxin, reduce the side effects of T-2 toxin and improve the inhibiting and killing effects of T-2 toxin on the tumor tissues.
US7608603 preferential enzyme inhibitors comprising fused pyrazolo pyrimidine derivatives used for treating arthritis, Crohns disease, irritable bowel syndrome, adult respiratory distress syndrome, or chronic obstructive pulmonary disease Compounds of formula Ia, Ib, Ic, Id, Ie, If, Ig or Ih: wherein X and Y are nitrogen or one of X and Y is nitrogen and the other is CRg, and W, D, E, R4, R5, R6 and Rg are as defined herein. Also disclosed are methods of making the subject compounds and methods of using the compounds in the treatment of p38 MAP kinase-mediated diseases.
US7138529 e.g., N-(3-Cyano-4,5-dimethyl-thiophen-2-yl)-2,2-diphenyl-acetamide;3-Methyl-2-phenyl-pentanoic acid-(3-cyano-5,6-dihydro-4H-cyclopenta[b]thiophen-2-yl)-amide; or N-(3-Cyano-6-methanesulfonyl-4,5,6,7-tetrahydro-thieno [2,3-c]pyridin-2-yl)-2,2-diphenyl-acetamide; The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4 and n are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the antagonism of the glucagon receptor, such as diabetes.
WO2010150612A1 Hyaluronic acid production promoter and melanin production inhibitor Disclosed are a hyaluronic acid synthesis promoter and a melanin production inhibitor. Each of the hyaluronic acid synthesis promoter and the melanin production inhibitor contains a soybean saponin as an active ingredient. It is preferred that the soybean saponin be a soybean saponin aglycon. It is also preferred that the soybean saponin aglycon contain soyasapogenol A and/or soyasapogenol B. The hyaluronic acid synthesis promoter and the melanin production inhibitor can be administered transdermally or orally.
EP1320522B1 Compositions and methods of the use thereof achiral analogues of cc-1065 and the duocarmycins The present invention relates to novel achiral seco-analogues of the DNA minor groove and sequence-selective alkylating agents (+)-CC1065 and the duocarmycins, depicted as general class (I), (II), (III), (IV) and (V) wherein X is a good leaving group, such as chloride, a bromide, an iodide, a mesylate, a tosylate, an acetate, a quaternary ammonium moiety, a mercaptan, an alkylsulfoxyl, or an alkylsulfonyl group, preferably either a chloride, a bromide, or an iodide group. R1 is a suitable minor groove binding agent to enhance the interactions of the achiral seco-cyclopropaneindole (CI) or an achiral seco-duocarmycin with specific sequences of DNA. R and R2-R5 are defined in claim 1.
EP1864983A1 Pyrimidine compounds as cyclin-dependent kinase inhibitors The present invention relates to substituted pyrimidines of formula (I), their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders.
CN101917991A Plastic container having cyclic polyolefin layer Disclosed are a multilayered film and a plastic container each of which comprises a heat-sealable seal layer, a cyclic polyolefin layer and an outermost layer, wherein the seal layer comprises a polypropylene, the cyclic polyolefin layer comprises a cyclic polyolefin polymer or a cyclic polyolefin copolymer and the outermost layer comprises a layer comprising a polypropylene, and wherein each of the multilayered film and the plastic container further comprises a resin composition layer comprising a blend of a propylene polymer and a styrene-type elastomer. The plastic container enables to prevent the reduction in the content of a medicinal agent in a liquid pharmaceutical preparation, and has excellent impact resistance, excellent handling properties during filling a material into the container, excellent moldability, and excellent transparency.
WO2008040057A1 Novel benzofuran potassium channel blockers and uses thereof The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
CA2312087C Preparation comprising sterically hindered amines for the prevention and treatment of inflammation A preparation for prevention and healing of inflammation affections comprising in an amount of 0.1 to 99.9 % by weight derivatives of sterically hindered amines selected from the group consisting of: soluble polymers or copolymers prepared by radical polymerization in the presence of 0.01 to 10 % by weight, of initiators prepared in a polymerization mixture comprising individually or in combination an aliphatic amine monomer of general formula (A), soluble polymers or copolymers prepared by radical polymerization in the presence of 0.01 to 10 % by weight of initiators from monomers of cyclic sterically hindered amines of general formula (B), soluble polymers prepared by polycondensation of difunctional sterically hindered amines of general formula (F), soluble polymers or copolymers prepared by polycondensation of difunctional cyclic sterically hindered amines of general formula (G), soluble copolymers prepared by polycondensation of difunctional cyclic, sterically hindered amines of general formula (G) and monofunctional cyclic sterically hindered amines in an amount of 0.1 to 15 % by weight, based on the total polymerization mixture, of general formula (H), derivatives of sterically hindered cyclic amines of general formula (O), polymers, copolymers, or natural compounds comprising free reactive groups -OH, -NH2, -COOH, -CHO, oxiranyl, selected from the group poly(vinyl alcohol), cellulose, (2-hydroxyethyl)cellulose, (carboxymethyl)cellulose, agar derivatives, polymers obtained by condensation, using alkanediol derivatives, oligomers and polymers of ethylene glycol or propylene glycol, natural or synthetic polymers, comprising a free carboxyl group, amino group or aldehyde group, prepared by additional functionalization of polymers or natural compounds by polymeranalogous reaction with a suitable sterically hindered amine.
WO2006106804A1 Tricyclic spiro compound comprising acyl group bound to nitrogen atom in the ring It is intended to provide an anticoagulant that has an extremely excellent FXa inhibitory action and an extremely weak hERG channel inhibitory action and can be orally administered, which is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.
US20130072565 Method of increasing cell proliferation by advanced wound dressings The present invention relates generally to a method for stimulating cell proliferation. More specifically this invention discloses the use of increased cell proliferation in treatment of certain wounds.
WO2014024119A1 Heterocyclic amides as itk inhibitors The present invention is directed to heterocyclic amide compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by ITK.
WO2005089804A3 Combinations of hmg-coa reductase inhibitors and alpha1 adrenergic receptor antagonists Combinations of an HMG-CoA reductase inhibitor, other than atorvastatin, and α1 adrenergic receptor antagonists, the use of such combinations in the treatment of benign prostatic hyperplasia (BPH), methods of treating BPH using such combinations and medicaments containing such combinations are described.
US20120058088 Resveratrol-Containing Compositions And Methods Of Use A resveratrol-containing composition capable of providing a therapeutic benefit to a subject such as modulation of a biological activity, improving cell transplantation therapy, or improving macular degeneration or dystrophy treatments. The compositions comprise trans-resveratrol, a metal chelator, and one or more additional antioxidants such as phenolic antioxidants or vitamin D.
CN103006594A Glimepiride composite and preparation method thereof The invention relates to glimepiride for treating diabetes mellitus, and a preparation method of glimepiride. A glimepiride tablet composite is characterized in that every 1000 tablets of composites comprise 2g glimepiride, 85g mannitol, 73.3g lactose, 6.8g sodium carboxymethyl starch, 1.2g povidone K30, and 1.7g magnesium stearate, wherein glimepiride adopts a micronization technique, and D90 is less than or equal to 4.0 micrometers. A glimepiride tablet with high dissolubility and stable performance is obtained.
US7256219 Multifluoro-substituted chalcones and analogs as activators of caspases and inducers of apoptosis and the use thereof The present invention is directed to multifluoro-substituted Chalcones and analogs thereof, represented by the general Formula I: wherein Ar and R6-R10 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
US20090264408 Extended release dosage forms of quetiapine The present invention relates to an extended release dosage form of quetiapine wherein the dosage form comprises quetiapine and rate-controlling polymer selected from polyethylene oxide, sodium alginate and natural gum and combinations thereof. The dosage form may additionally comprise at least one water-insoluble polymer.
WO2007072216A3 Kit and composition of imidazole with enhanced bioavailability A composition and therapeutic kit provide a therapeutic azole with increased solubility. The kit includes an aerosol packaging assembly containing a container accommodating a pressurized product and an outlet capable of releasing the pressurized product as a foam. The pressurized product includes a foamable composition including: i. a therapeutic azole, wherein the solubility of the azole in the composition before foaming is less than the solubility of the azole in the composition after foaming; ii. at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, a co-solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 50% by weight; iii. a surface-active agent; iv. about 0.01% to about 5% by weight of at least one polymeric additive selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent and a phase change agent; v. water; and vi. liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition.
CN1939268A Oral preparation containing azithromycin and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains azithromycin. Its preparing process is also disclosed.
CN101708184B Medicine application of iron liposome The invention discloses a medicine application of iron liposome. By taking animals with chronic inflammation as a model, a brand-new medicine which treats anaemia caused by the dysfunction of the iron absorption of the small intestine to relevant protein molecules and takes the iron liposome as an effective component is provided. The invention takes white rats with inflammatory anaemia as a model, adopts an oral stomach infusion method and compares the curative effect of the iron liposome for the anaemia with that of a chalybeate which is not enveloped by the liposome, and the iron liposome can obviously enhance the levels of the hemoglobin, the blood cell volume, the serum iron and the saturation rate of the transferrin of an organism in a short time, can act as a very good curative effect to the inflammatory anaemia and can not cause injuries to the health of the organism. The iron liposome is obviously superior to the traditional iron-replenished preparation. The invention can be used for treating the anaemia caused by the dysfunction of the iron absorption of the small intestine to the protein molecules because of various known or unknown reasons. Various tablets, capsules, dripping pills, oral liquid and food additives which are taken orally and contain the iron liposome are prepared.
CN103182085A Methods and compositions for cellular drug release Methods and compositions for producing a cellular drug release are disclosed. The method comprises: a) providing a composition comprising a therapeutically effective amount of a pharmacological agent adsorbed onto mesoporous hydroxyapatite (HAP) with hydrophobic surfaces; b) exposing the composition to a cell; c) causing entry of the mesoporous HAP into the cell and degradation of the HAP in the lysosomes of the cell and desorption of the agent from the mesoporous HAP; d) causing release of the desorbed agent from the lysosomes into the cytoplasm of the cell; and e) causing release of the desorbed agent to outside the cell. The composition comprises a) mesoporous HAP with hydrophobic surfaces; and b) a therapeutically effective amount of a pharmacological agent, adsorbed onto the hydrophobic surfaces of the mesoporous. HAP. The composition is characterized in that it constantly releases the agent in vivo for a period of at least 4 weeks.
EP1157006B1 Phenyl- and pyridinyl derivatives as neurokinin 1 antagonists The invention relates to compounds of general formula (I), wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together -CH=CH-CH=CH-; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is independently from each other hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, halogen, lower alkyl, lower alkoxy, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R?5)C(O)R5¿ or a cyclic tertiary amine of the group (a); R5 is, independently from each other, hydrogen, C¿3-6?-cycloalkyl, benzyl or lower alkyl; R?6¿ is hydrogen, hydroxy, lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R5)-, -(CH¿2?)mO-, -(CH2)mN(R?5¿)-, -N(R5) C(O)-, C(O)O- or -N(R5)(CH2)m-; Y is -(CH2)n-, -O-, -S-, SO2-, -C(O)- or -N(R5)-; Z is =N-, -CH= or -C(C1)=; n is 0 - 4; and, is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formula (I) have a high affinity to the NK-1 receptor.
CN101255180A Diphenyl ethylene glycosides derivatives The invention relates to a new type 2, 3, 5, 4'- tetra-hydroxyl diphenyl ethylene-2-O-beta-D-glucoside crystal, a method for making same, and pharmaceutical compositions containing the crystal. The content of the crystal is 90-99. 9tested by high performance liquid chromatography, and the stilbene glucoside crystal of high-purity is obtained by abstracting fleece-flower root, extracting with an organic solvent, separating by column chromatography and crystallizing in appropriate dissolvent. The preparing process provides high yield, low cost, and is suitable for industrial production.
CN1903194A Slow-release, controlled-release prepn. of simvastatin, and method for preparing same A slow-releasing or release-controlled simvastatin contains proportionally simvastatin, C3-20 aliphatic carboxylic acid and/or alditol, one or more of carboxypropyl methylcellulose and/or sodium alginate, stearic acid, and vinyl acetate-polyvidone, one or more of dextrin, starch, carboxymethyl starch, lactose, calcium hydrogen phosphate and microcrystalline cellulose, and lubricant. Its preparing process is also disclosed.
US20080241151 Neisserial peptides for use in developing vaccine for prevention and treatment of menigococcal septicemia and meningitis A series of genes from Neisseria meningitidis are shown to encode products which are implicated in virulence. The identification of these genes therefore allows attenuated microorganisms to be produced. Furthermore, the genes or their encoded products can be used in the manufacture of vaccines for therapeutic application.
WO2011055944A2 Methods for treating fibromyalgia syndrome The invention is directed to a method of treating fibromyalgia syndrome in a subject, comprising administering a therapeutically effective amount of a carbamoyl compound, or pharmaceutically acceptable salt thereof.
US20110311466 Novel 4-(azacycloalkyl)benzene-1,3-diol compounds as tyrosinase inhibitors, process for the preparation thereof and use thereof in human medicine and in cosmetics 4-(azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.
EP2758063A1 Use of klinoptilolith or klinoptilolith-containing mixtures for producing medicinal products The invention relates to the use of klinoptilolith or klinoptilolith-containing mixtures for producing medicinal products or other pharmaceutical products, for the absorption and removal of caesium ions from the human or animal organism. Here, the klinoptilolith is modified by purification and comminution. The products are suitable, when taken in a preventative and/or timely manner, for reducing both the concentration of the absorption of radioactive caesium ions and also of non-radioactive caesium ions into the human or animal body. The medicinal product or pharmaceutical product is likewise suitable for reducing the caesium ions already present and absorbed in the living being when taken over a certain period, stepwise in the concentration after they have been taken.
WO2005120522A1 Rheumatism preventive or therapeutic agent and beverage each comprising reduced-deuterium water A preventive or therapeutic agent for rheumatism that being free from side effects as brought about by steroids, methotrexates, gold preparations, etc., excels in safety and is capable of realizing the prevention and treatment of rheumatism in a simple manner. Further, there are provided, ingested for the prevention and treatment of rheumatism, a beverage, soft beverage, health beverage, beverage for specified health use, food, health food and food for specified health use. In particular, there is provided a rheumatism preventive or therapeutic agent, or beverage, or food comprising reduced-deuterium water as an active ingredient. These agent, beverage and food would attain the prevention and treatment of rheumatism through drinking of a given amount of reduced-deuterium water, especially reduced-deuterium water of 0 to 100 ppm deuterium concentration, for a given period of time, or through ingestion of food having the reduced-deuterium water incorporated therein.
CN101511369B Methods and compositions for inhibiting angiogenesis. The present invention relates to a method of inhibiting angiogenesis in a biological system. The method includes administering to the biological system an effective amount of a steroid saponin.
CN102895257A Compound triclocarban complex iodine disinfectant and preparation method thereof The invention discloses a compound triclocarban complex iodine disinfectant, which consists of the following raw materials in percentage by weight: 0.1-1 percent of triclocarban, 0.5-10 percent of povidone iodine, 20-50 percent of isopropanol, 5-20 percent of a nonionic surfactant, 0.05-0.2 percent of a stabilizing agent and the balance of distilled water. The compound disinfectant is a reddish brown transparent liquid, has high stability, contributes to preventing the production of drug-fast bacteria, and has the characteristics of safety, quick response, long acting and the like; and the antimicrobial spectrum range is expanded, and the defects of single-component disinfectants are overcome.
CN1608669A Filming aerosol for treating tinea coporis, tinea manuum and tinea pedis The filming aerosol for treating tinea coporis, tinea manuum and tinea pedis is prepared with salicylic acid, Clotrimazole, phenol, camphor, wintergreen oil, glycerin and alcohol, and through conventional preparation process. The present invention has the advantages of being convenient, clean and high in healing rate. The medicine liquid forms film on skin, and this can prevent volatilization of medicine component, last effect and avoid contamination to clothing. In addition, the medicine liquid has lauryl azatroketone as transdermal promoter added and has thus fast release of medicine component, strengthened absorption of skin to medicine and high curative effect.
US20110257074 Method for the purification of substituted cyclopent-2-en-1-one congeners and substituted 1,3-cyclopentadione congeners from a complex mixture using countercurrent separation Methods of purifying individual congeners of substituted cyclohexa-2,4-dienones, substituted cyclohexane-1,3,5-triones, substituted cyclopent-2-en-1-ones, and substituted 1,3-cyclopentadiones and compositions using the same are disclosed. The purification method includes the steps of: (a) selecting a congener to be isolated; (b) dissolving the mixture of congeners in a bi-phasic solvent system specific to the selected congener to be isolated, wherein said bi-phasic system has a partition coefficient from about 0.5 to 5.0; (c) subjecting the mixture dissolved in the bi-phasic solvent system to a counter current chromatography; and (d) isolating the selected congener in substantially pure form.
US8058267 Steroids as agonists for FXR The invention relates to compounds of formula (I): wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
CN101289408A Non-steroid progestogen receptor regulator, preparation thereof, pharmaceutical compositions and uses The invention relates to a modulator of nonsteroidal progesterone receptor with a structure of the general formula I or an acceptable salt on pharmacy and a preparation method thereof. The invention also relates to drug combination including compounds of the general formula I or an acceptable salt on pharmacy thereof and the antagonist activity of progesterone receptor which is provided by the compounds of the general formula I or the acceptable salt on pharmacy thereof; therefore, the invention can be used for preparing nonsteroidal drugs to prevent and (or) or treat symptoms or diseases such as secondary amenorrhea, functional bleeding disorder, uterine fibroids, endometriosis, polycystic ovary syndrome, breast cancer, contraceptive, induced labor, and termination of pregnancy, etc.
CN1935186A Compound perillaseed oil and its capsule pill The present invention belongs to the field of medicine and health-care product for cardiovascular system. In the concrete, it relates to a compound perilla seed oil and its capsule preparation. It can be used for preventing and curing the diseases of hypertension, hyperlipemia and angiocardiopathy. Its composition contains (by wt%) 0.01-0.05% of vitamin C, 0.03-0.12% of water. 0.1-0.5% of vitamin E and the rest is perilla seed oil.
US20080044409 Inflammatory mediator antagonists The present invention relates to methods of reducing cartilage degradation in a patient comprising administering to a patient in need thereof an effective amount of an antibody antagonist to the mature form of OSM.
CN102079761A Water-soluble S, S-heptaplatin derivative The invention relates to a new water-soluble S, S-heptaplatin derivative-cis-[(4S, 5S)-4, 5-bi (aminomethyl)-2-isopropyl-1, 3-dioxolane 3-hydroxy-1, 1-cyclobutanedicarboxylate platinum (II)]. The derivative is prepared by the following steps of: (1) preparing a required amine ligand by using L-diethyl tartrate as an initial raw material through condensation, ammonolysis and LiAlH4 reduction reaction; and (2) adding LI to K2[PtCl4] used as an initial raw material, transforming the raw material into K2PtI4, making the K2PtI4 react with the amine ligand (4S, 5S)-4, 5-bi (aminomethyl)-2-isopropyl-1, 3-dioxolane to prepare a corresponding diiodo intermediate, and making the diiodo intermediate react with 3-hydroxy-1, 1-cyclobutanedicarboxylate in equimolar amounts to obtain a target compound. The compound has the characteristics that the antitumaous effect of the compound is higher than that of carboplatin, heptaplatin and R, R-derivatives thereof, and the toxicity is lower than that of carboplatin, heptaplatin and R, R-derivatives thereof. The compound can be used for treating cancers clinically. Moreover, the compound also has the advantages of good water solubility and stability, and can be prepared into lyophiled powder or aqueous solution.
US7053068 Chitosan-thio-amidine conjugates and their cosmetic as well as pharmaceutic use By the reaction of chitosan with iminothiolactones such as 2-iminothiolane, thiol groups can be covalently immobilized on the polymer. The resulting chitosan derivatives exhibit thiol groups which are capable of forming inter- and intramolecular disulfide bonds. Because of this crosslinking process the viscosity of polymer solutions is strongly improved. Moreover, the cationic character of the polymer is strongly improved. Preferred applications of these novel chitosan derivatives are their cosmetic and pharmaceutical use
US20100015093 Methods and compositions of treating a flaviviridae family viral infection Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3′UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.
US20080108679 Isoxazolic Derivative to Relieve Neuropathic Pain The present invention relates to new pharmaceutical uses of an isoxazolic derivative or a pharmaceutically acceptable salt thereof in the preparation of a medicament useful for treating the neuropathic pain.
WO2014043144A1 Methods for treating inflammation and pain The present invention is directed to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and an ω-(methanesulfonyl)alkenylnitrile compound, or a pharmaceutically acceptable salt thereof. The present invention is also directed to a method for treating inflammation, inflammatory-related disorders, or pain, by orally administering an ω-(methanesulfonyl)alkenylnitrile compound or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.
WO2007048803A1 Benzimidazolone derivatives for the treatment of premenstrual and other female sexual disorders The invention relates to the use of benzimidazolone derivatives of formula (I) for the preparation of a medicament for the treatment of premenstrual and other female sexual disorders.
WO2011039381A1 Antioxidants for use in therapy Compounds based on the followining structures: wherein each of R1, R2, R3 and R4 is independently selected from: hydrogen, alkyl, and substituted alkyl; and each of R5, R6 and R7 is independently selected from: hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, N,N-dialkylamino, substituted N,N-dialkylamino, N-monoalkylamino, substituted N-monoalkylamino, and electron-donating substituents are useful in the treatment of disorders or conditions caused by or involving free radical-mediated or oxidative tissue damage.
CN101698017A Antiphlogosis and sterilizing ointment The invention provides an antiphlogosis and sterilizing ointment with favorable effects of treating eczema, dermatitis and other intractable skin diseases. The antiphlogosis and sterilizing ointment is prepared by the following steps: using red orpiment, Cinnabaris, borneol, borax (stir-fried), natrii sulfas exsiccatus, dittany bark, broom cypress fruit, angelica dahurica, Chinese rhubarb, Fructus Forsythiae and phellodendron as the raw materials, leaching the effective components from the drugs by using a proper solvent, and evaporating all or part of the solvent until the concentration of glycerin reaches the specified standard and the water content reaches 15-20%. The bioactive components not only can effectively improve the symptoms of skin itch, gall, furfuration, roseola and the like, but also has the effects of relieving itching and pains, clearing heat for detoxication, diminishing inflammation, sterilizing and removing tumescence, and has favorable curative effects for most severe skin diseases. Compared with the prior art, the invention is safe and effective and does not have any side effect on human body.
WO2012136099A1 4-(substituted phenylamino)quinazoline derivative and preparation method therefor, pharmaceutical composition and use thereof The present invention relates to a 4-(substituted phenylamino)quinazoline derivative and a preparation method therefor, a pharmaceutical composition and a use thereof. In particular, the present invention relates to a compound of formula I or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2 and R3 are as defined in the specification and claims. The present invention further relates to a method for preparing the compound of formula I, a pharmaceutical composition comprising the compound and pharmaceutical uses of the compound and pharmaceutical composition. The compounds of formula I according to the present invention are potent irreversible inhibitors of tyrosine kinases.
WO2010149658A3 Pharmaceutical composition comprising gamma - butyrobetaine and meldonium Pharmaceutical composition of gamma-butyrobetaine and Meldonium dihydrate and its use in prevention and/or treatment of atherosclerosis and/or neurological diseases.
WO2011135259A1 Pyrido[3,2-d]pyrimidine derivatives, processes for preparing same and therapeutic uses thereof The present invention relates to a compound of following general formula (I): (I) in which: - R1 is in particular H, a halogen atom or an aryl group, - R2 is in particular a halogen atom or an aryl group, - R3 is in particular a halogen atom or an aryl or heteroaryl group, and also the pharmaceutically acceptable salts thereof, the hydrates thereof or the polymorphic crystalline structures thereof, the racemates, diastereoisomers or enantiomers thereof, with the exception of the compound 1‑C2,4-diaminopyrido[3,2-d]pyrimidin-7-yl)-3,6,6-trimethyl-6,7-dihydro-1H-indol-4(5H)-one.
US20080255206 Rxr Agonists and Antagonists, Alone or in Combination with Ppar Ligands, in the Treatment of Metabolic and Cardiovascular Diseases The present invention relates to the use of one or more retinoid agonists and/or antagonists comprising retinoids with selective Retinoid X Receptor (RXR) agonistic or antagonistic activity alone or in combination with one or more peroxisome proliferator activated receptor (PPAR) ligands for the manufacture of a medicament for the (preferably oral or topical) treatment (this term including prevention/prophylaxis and/or therapy) of one or more manifestations of metabolic syndrome (also known as syndrome X), also called diseases hereinafter, especially from one or more manifestations thereof selected from the group consisting of diabetes type II, obesity, dyslipidemia, hypertension and polyneuropathy, each of which can also be linked with a high risk of cardiovascular diseases. Corresponding methods, the compounds and combinations for use in the treatment of the mentioned diseases and comparable invention embodiments are also described.
CA2164061C Cosmetic compositions containing lactate dehydrogenase inhibitors Inhibitors of lactate dehydrogenase stimulate keratinocyte proliferation and collagen synthesis in cutaneous tissues. The inhibitors are used preferably with certain co-active ingredients such as pyruvic acid, acetic acid, acetoacetic acid, .beta.-hydroxybutyric acid, a Krebs cycle pathway metabolite, an aliphatic saturated or an unsaturated fatty acid containing from 8 to 26 carbon atoms, an a-hydroxy acid containing from 22 to 34 carbon atoms, glutamic acid, glutamine, valine, alanine, leucine, and mixtures thereof.
US20120264770 Hsp90 inhibitors The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
CN101898961A Parietic acid crystal C type solid matter as well as preparation method and application thereof The invention discloses a C type solid matter state of a parietic acid compound shown as the formula (I), a preparation method of a crystal A type solid matter sample of the parietic acid compound as well as a medicament and a medicament composition which are prepared and developed by adopting the A type solid matter as medicament active ingredients, wherein the medicament and the medicament composition take better clinical effects in preventing and treating diseases.
CN103038234A Compounds with antibacterial activity against clostridium The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
CN103211829A Compounds having virus resistance and composition thereof The invention discloses compounds having virus resistance and a composition thereof. The composition comprises one or more of the 13 compounds comprising 6'-O-caffeoyl deacetyl asperulosidic acid methyl ester. The compounds having virus resistance and the composition thereof can be extracted from plants and can also be prepared by synthesis. The composition comprising the compounds having virus resistance can prevent and treat viral infection-caused diseases such as influenza, myocarditis, conjunctivitis, viral pneumonia, encephalitis, leukemia, hepatitis B, hepatitis C, AIDS, genitourinary system infection, EB virus infection, human papillomavirus infection and cytomegalovirus infection. The composition can be prepared into an oral preparation, an injection, a spray, a subcutaneous injection and an anus suppository.
US20080058356 2,6 Bisheteroaryl-4-Aminopyrimidines as Adenosine Receptor Antagonists 4-Aminopyrimidine derivatives of formula (I) FORMULA heteroaryl groups, including pharmaceutically acceptable salts thereof, wherein R1 and R2 are adenosine A2A receptor antagonists useful in the treatment of movement disorders such as Parkinson's disease.
US7414034 Administering antibody polynucleotide; controlling glutamate receptors The present invention relates to a method of treatment of Parkinson's disease, and to the use of antisense oligonucleotides or triplex oligonucleotides introduced into targeted brain structures to decrease the function of brain circuits known to be overactive in the Parkinsonian brain. Antisense or triplex oligonucleotides are targeted to the internal globus pallidus and/or substantia nigra pars reticulata (SNr) where the expression of glutamic acid decarboxylase (GAD67, GAD65, or a combination of the two isoforms) is downregulated. The present invention also relates to a method of treatment of Parkinson's disease where antisense or triplex oligonucleotides are targeted to the internal globus pallidus and/or substantia nigra pars reticulata for the downregulation of glutamate receptors. The present invention further relates to a method of treatment of Parkinson's disease where antisense or triplex oligonucleotides are targeted to the thalamic motor nuclei for the downregulation of GABA receptors.
CN102892750A Process for the preparation of chiral hydrazides The present invention relates to a process for the preparation of a chiral compound according to formula (V) wherein R1 is preferably an alkyl residue preferably having from 1 to 6 carbon atoms, in particular to a process for the preparation of a chiral compound the crystalline chiral compounds as such, and their use for the preparation of an antifungal agent, in particular posaconazole.
CA2804599A1 Mirna and its diagnostic and therapeutic uses in diseases or conditions associated with melanoma, or in diseases or conditions associated with activated braf pathway The invention relates to the diagnostic and therapeutic uses of a miRNA molecule, an equivalent or a source thereof in a disease and condition associated with melanoma or a disease or a condition associated with activated BRAF pathway.
CN103372025A Face cleaning paste The invention belongs to the technical field of medicine science, and discloses a face cleaning paste. According to the background technology, realgar and jade pieces have an acarid repelling and killing function, and the face cleaning paste is prepared by taking the realgar and the jade pieces as main components. The face cleaning paste provided by the invention belongs to an external use paste and does not have a view. The face cleaning paste comprises the specific implement steps of: uniformly mixing 19 grams of realgar,10 grams of jade pieces, 6 grams of alum and 10 grams of vaseline to form paste, and bottling the paste for standby coating.
CN103655608A Preparation method of external use medicament for treating oral ulcer The invention discloses a preparation method of an external use medicament for treating oral ulcer. The preparation method comprises the following steps: a, mixing 5-15g of alum and 2-8g of white sugar; b, putting the mixture of the step a into a heatable container to be heated for 2-5 minutes at the temperature of 50-80 DEG C; and c, cooling the medicament which is heated and molten in the step b to be normal temperature, and sealing up to store. The external use medicament is reasonable in composition, convenient to take, free of toxic and side effects, capable of effectively treating oral ulcer and eliminating the disease from patients.
US20080176873 Novel Pharmaceutical Compositions for Treating Acquired Chronic Pain and Associated Dysphoria Chronic pain is alleviated in a mammal suffering there from by administering to the mammal a chronic pain alleviating amount of a nontoxic N-methyl-D-aspartate receptor antagonist such as dextromethorphan, dextrorphan, ketamine or pharmaceutically acceptable salt thereof, in combination with a μ-opiate analgesic such as tramadol or an analogously acting molecular entity, and a methylxanthine such as caffeine, and optionally in sustained release dosage form.
US20100168138 Anti-Viral Compounds Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
WO2008046407A2 Use of deuterium dioxide for treating hyperproliferative skin diseases The invention relates to D2O and the use thereof for producing a medicament for the prophylaxis and/or treatment of hyperproliferative skin diseases. The invention also relates to plasters, bandages, aerosols and formulations.
US20100112087 Oxygen-generating compositions for enhancing cell and tissue survival in vivo A method of treating hypoxic tissue such as wound tissue comprises contacting a composition to the hypoxic tissue in a hypoxia-treatment effective amount, the composition comprising a biodegradable polymer and an inorganic peroxide incorporated into the polymer.
US7084128 Administering purinerginic receptor ligand, which is a mononucleoside polyphosphate or dinucleoside polyphosphate such as di-5'-((2'O-benzyl)adenosine)tetraphosphate; for treatment of glaucoma The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a purinerginic receptor ligand, which is a mononucleoside polyphosphate or dinucleoside polyphosphate defined by general Formula I. The method of the present invention is useful in the treatment or prevention of ocular hypertension, such as glaucoma, including primary and secondary glaucoma. The method can be used alone to reduce intraocular pressure. The method can also be used in conjunction with other therapeutic agents or adjunctive therapy commonly used to treat glaucoma to enhance the therapeutic effect of reducing the intraocular pressure.
US7087588 to gastrointestal systems, kidneys Use of organic compounds containing the —ONO2 function, or inorganic compound containing the —NO group or compositions comprising said compounds to reduce the toxicity caused by drugs to the gastrointestinal and/or renal apparatus, said compounds being characterized in that they are nitric oxide NO donors i.e., when they are put into contact in vitro with cells of the vasal endothelium or platelets.
CN101607091A Method for synthesizing dextran-magnetic LDH-fluorouracil magnetic targeting sustained and controlled release tripolymer The invention relates to a method for synthesizing dextran-magnetic LDH-fluorouracil magnetic targeting sustained and controlled release tripolymer, comprising the following steps of: finishing the synthesis of magnetic layered composite hydroxide and the intercalation assembly of fluorouracil to the magnetic layered composite hydroxide under the condition of nitrogen protection; performing the in-situ composite process of magnetic LDH-fluorouracil under the condition of nitrogen protection with the dextran as the wrapping material; and finally separating the product through the solvent conversion technology. The invention realizes the merging and unification of the targeting and the sustained release of a magnetic targeting drug, thereby solving the problems of the preparation of magnetic LDH-Drugs and protection against oxidation, and synthesizing a magnetic targeting sustained and controlled release drug delivery system which has good biocompatibility and high storage stability and fits for transport in vivo; and the invention is suitable for the chemical synthesis of various magnetic targeting sustained and controlled release drugs, and has the advantages of simple and rapid preparation technology, high product purity, energy consumption saving, no environment pollution, wide application range and the like.
US7271184 For controlling parasites on warm-blooded animals; veterinary medicine Novel pesticides of formula (I) wherein the substituents, R, R1, R2, R2′, T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as parasiticides comprising those compounds as active ingredient and to methods of controlling parasites that are based on the administration of those compounds or compositions, and to the use of the said compounds and compositions in a method of controlling parasites and in the manufacture of pesticides for use against parasites. Also described are intermediates of formula (XX) wherein R1, R2, R2′, T, U, X and Y are as defined in claim 1; and Hal is halogen. The latter also exhibit parasiticidal activity and are suitable for the preparation of the compounds of formula (I).
US20090004191 Expansion of Stem/Progenitor Cells by Inhibition of Enzymatic Reactions Catalyzed by the Sir2 Family of Enzymes Provided are ex vivo and in vivo methods of expanding renewable stem cells using agents capable of down-regulating Sir2 protein activity and/or expression, expanded populations of renewable stem cells, and uses thereof.
CN101679260A 4,4-disubstituted piperidine derivatives This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
US8263394 Polynucleotides encoding antigenic HIV type B polypeptides, polypeptides, and uses thereof The present invention relates to polynucleotides encoding immunogenic HIV polypeptides. Uses of the polynucleotides in applications including immunization, generation of packaging cell lines, and production of HIV polypeptides are also described. Polynucleotides encoding antigenic HIV polypeptides are described, as are uses of these polynucleotides and polypeptide products therefrom, including formulations of immunogenic compositions and uses thereof.
CN103655490A Idarubicin hydrochloride pharmaceutical composition and preparation method thereof The invention discloses idarubicin hydrochloride pharmaceutical composition and a preparation method thereof. The composition contains idarubicin hydrochloride and mannitol. The preparation method comprises the following steps: 1), preparation is performed: ambroxol hydrochloride and mannitol are placed into a preparation tank in a weight ratio of 1:(1-20), water for injection is added, and the mixture is stirred to be completely dissolved and uniformly mixed; 2), sterile filtration, subpackaging and half stoppering are performed; and 3), vacuum freeze drying is performed to obtain a product. The composition and the preparation method have the advantages that the formula is simple, the technology is advanced, the quality is uniform and stable, moisture is thoroughly dried, and the redissolution performance is better.
US20120238629 Addition compounds of guanidinoacetic acid The present invention provides new addition compounds of guanidinoacetic acid with malic acid, aspartic acid, ascorbic acid, succinic acid, pyruvic acid, fumaric acid, gluconic acid, alpha-ketoglutaric acid, pyroglutamic acid, 3-nicotinic acid, lactic acid, citric acid, maleic acid, acetic acid, formic acid, 2-hydroxybenzoic acid, L-carnitine, acetyl-L-carnitine, taurine, betaine, choline, methionine and lipoic acid as well as in the form of sodium, potassium or calcium guanidinoacetate. These addition compounds have improved physiological and therapeutic properties and are particularly suitable for use as dietary supplements, as animal feeds and in cosmetic or dermatological preparations in which especially the marked stability and good bioavailability of the addition compounds come to the fore.
WO2009112529A1 Novel method for the production of sulphonylpyrroles as hdac inhibitors Process for the preparation of a compound of formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, comprising the step of reacting an acrylic acid chloride compound of formula (II'): wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, with aqueous hydroxylamine and optionally converting the resulting compound into an acid addition salt thereof.
CA2637418A1 Serotonergic agents for treating sexual dysfunction Methods and compositions are provided for treating sexual dysfunction, e.g., sexual dysfunction associated with drug treatment, using 5-HT1A receptor antagonists.
CN101028278A Medicinal effect of psilotopsida glucoside against cancers An application of the psilopsida or its glycoside in preparing anticancer medicine is disclosed.
CN1803129A Sodium diclofenac mucilage The invention provides a novel dosage form of diclofenac sodium for analgesic and pain-relieving, wherein a rectal intestine administration mode is employed for preventing stimulations to gastrointestinal tract and accelerate absorption.
US20110064683 Personal care compositions with ethylene acrylic acid copolymer aqueous dispersions Described are personal care compositions, comprising an aqueous dispersion comprising an ethylene acrylic acid copolymer and a least one cosmetically acceptable surfactant, emollient, or cosmetic active.
WO2009064082A1 Composition comprising galla rhois extract for prevention and treatment of obesity by means of autophagic mechanism The present invention relates to a composition comprising a Galla Rhois extract for the prevention and treatment of obesity based on the mechanism of autophagocytosis. In particular, the present invention has found that the Galla Rhois extract or fraction thereof exhibits inhibitory effects on the proliferation of adipocytes by inducing autophagocytosis thereof, and therefore, provides a method of isolating active ingredients capable of being used as a composition for the prevention and treatment of obesity from Galla Rhois, and a composition for the prevention and treatment of obesity which comprises a Galla Rhois extract or a fraction thereof. That is, the Galla Rhois extract according to the present invention exerts beneficial activities of inducing autophagocytosis of adipocytes in vitro, inhibiting body weight gain in an obesity-induced animal model, reducing the body weight of a body weight gain-induced animal model, and lowering the levels of triglycerides and low density lipoproteins in the blood. Therefore, the Galla Rhois extract according to the present invention can be effectively used as a pharmaceutical composition and health foods for the prevention of obesity and complications thereof and treating the same.
CN101605547A Methods of treating chronic inflammatory diseases using a GM-CSF antagonist The invention is based on the discovery that GM-CSF antagonists can be used for the treatment of chronic inflammatory disease, such as rheumatoid arthirtis. Accordingly, the invention provides methods of administering a GM-CSF antagonist, e.g., a GM-CSF antibody, and an anti-folate compounds, e.g., methotrexate, to a patient that has RA and pharmaceutical compositions comprising such antagonists.
US8252766 Use of spongosine for the treatment of pain The compound spongosine (2-methoxyadenosine), of the class of adenosines, is useful as an analgesic, particularly in a method of preventing, treating, or ameliorating pain which comprises administering spongosine (2-methoxyadenosine) to a subject in need of such prevention, treatment, or amelioration.
WO2011034362A9 Composition containing saururus chinensis extract or sauchinone as an active ingredient, for preventing and treating diseases caused by the overexpression of lxr-α The present invention relates to a composition containing Saururus chinensis extract or Sauchinone as an active ingredient, which inhibits the expression or activity of liver X receptor α (LXRα) or sterol response element binding protein-1 (SREBP-1), and which can thus be used in preventing, improving, and treating diseases caused by the overexpression or activity of LXRα or SREBP-1. The composition of the present invention exhibits remarkable effects of inhibiting adipogenic gene expression, and further inhibiting the accumulation of triglycerides in liver tissue, and therefore is advantageous in treating fatty liver caused by metabolic disorders resulting from a high-fat diet. In addition, the composition of the present invention can be effectively used in preventing, improving, and treating, for example, liver diseases such as fatty liver caused by the accumulation of liver lipids, hypertriglyceridemia, hyperreninemia, renin-induced hypertension, aldosteronism, adrenoleukodystrophy, glomerulosclerosis, proteinuria, renal failure, etc.
EP2390327A1 siRNA and their use in methods and compositions for the treatment and/or prevention of eye conditions The invention relates to methods and compositions for the treatment/and or prevention of eye consitions related to high levels of expression and/or activity of the vanilloid-1 receptor (TRPV).
US20100190753 Methods and Compositions for Treating Amyloid-Related Diseases Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.
WO2013146943A1 Anti-aging agent containing arctigenin derivative An arctigenin derivative is created and used for anti-aging treatment, including in order to protect skin from the sun and to recover skin elasticity. A variety of fatty acid ester derivatives, alcohol ether derivatives and alkylated derivatives are created as the arctigenin derivatives. Agents for controlling ET-1 production, elastase inhibitors, and anti-inflammatory agents are prepared. Such arctigenin derivatives are particularly useful as an external agent for the skin, such as an anti-inflammatory external agent for the skin, a sunscreen external agent for the skin, or an external agent for the skin for recovering elasticity.
EP2422849A1 Composition of Indole-3-carbinol and either catechin, kaempherol, myricetin or luteolin for potentiating antitumour effect and for treating tumours Novel pharmaceutical composition of treating cancer, preferably malignant cancer by way of enteral use have been described, which contain Indole-3-carbinol and one of natural flavonoid derivative, preferably (+)-Catechin, Kaempferol, Myricetin or Luteolin.
US20060135471 Anti-obesity compositions The present invention relates to compositions and methods for treating obesity. More particularly, the invention relates to a composition comprising a lipase inhibitor such as orlistat, and glucomannan such as konjac as well as methods for utilizing such compositions and kits for carrying out this method.
EP0932388B1 Dosage form and method for administering drug A dosage form and a method are disclosed and claimed for administering a drug in a sustained and constantly ascending rate per unit time to provide an intended therapeutic effect while concomitantly lessening the development of unwanted effects.
WO2007036781A1 Diphenyl ether monoamine reuptake inhibitor The present invention relates to a compound of the formula (I) wherein R1 is hydrogen or C1-C6 alkyl; X and Y are independently selected from the group consisting of fluoro, chloro and bromo; its enantiomers, racemate and mixtures of enantiomers and the pharmaceutically acceptable salts thereof, which exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and are therefore useful in the treatment of central nervous system and other disorders.
US7151097 Bicyclic pyrazolyl and imidazolyl compounds and uses thereof Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals.
CN101816797A Gold nanoparticles used as medicament carrier and method for preparing same The invention discloses gold nanoparticles used as a medicament carrier and a method for preparing the same. The gold nanoparticles are characterized in that: membrane-penetrating peptides are combined on the surfaces of the gold nanoparticles through mercapto by forming covalent bonds, and the membrane-penetrating peptides are also combined with the carboxyl groups of pro-medicaments of platinum-based medicaments through amino by forming amido bonds; the membrane-penetrating peptide is a peptide fragment which has 8 to 20 amino acids including 1 cysteine and 5 to 19 arginines; the pro-medicaments of platinum-based medicaments are pro-medicaments of cisplatin, carboplatin, or oxaliplatin; the pro-medicaments of the cisplatin are selected from compounds 1,2 and 3; the pro-medicaments of the carboplatin are selected from compounds 4,5 and 6; and the pro-medicaments of oxaliplatin are selected from compounds 7,8 and 9. The gold nanoparticles connecting the platinum-based medicaments and the membrane-penetrating peptides have obviously-enhanced toxicity to tumor cells, and the gold nanoparticles not connected with the platinum-based medicaments are non-toxic. In the invention, a new route is opened up for the application of the gold nanoparticles in the biomedical field.
CN103222966A Solid pharmaceutical composition containing Fingolimod hydrochloride and preparation method thereof The invention belongs to the technical field of medicine, and concretely relates an oral pharmaceutical composition and a preparation method. The oral pharmaceutical composition comprises micronized fingolimod or pharmaceutically acceptable salts and pharmaceutically acceptable carriers thereof, and is existed in solid oral dosage forms such as tablets and capsules. The method is simple is preparation technology and suitable for industrial production; and the pharmaceutical composition can be used for treating multiple sclerosis, reduces frequency of clinical exacerbations and delays accumulation of physical disability.
US20110021483 Platinum (IV) Complexes Provided are nitroplatinum(IV) complexes containing a bidentate dicarboxylate ligand (e.g., oxalate) which maybe useful treating various forms of proliferative diseases, such as cancer. In some instances the platinum(IV) complexes are relatively stable and may be suitable for oral administration. Also provided are methods of treatment, as well as kits and unit dosages.
WO2008135526A1 Carboxylic acid amides as factor xa inhibitors The present invention relates to new substituted carboxylic acid amides of general formula (I), wherein D, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
US7026311 Dibenzodiazepine derivatives, their preparation and use The invention relates to compounds of the formula I and their tautomeric forms, possible enantiomeric and diastereomeric forms and their prodrugs, and to their preparation and use, where A, B, R1 and X1 have the meanings given in the description.
CN102858766A Polymorphs of a metabotropic glutamate receptor positive allosteric modulator Polymorphs of 7-methyl-5-(3-piperazin-1-ylmethyl-[l,2,4]oxadiazol-5-yl)-2-(4-trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-one mesylate salt, methods of making these polymorphs and uses thereof.
US20110178106 5-quinolinone and imidazopyridine compounds and use thereof 5-Quinolinone and Imidazopyrimidine compounds are provided that are useful for inhibiting the efflux of any therapeutic agent that is a MRP1 substrate. Also provided is a method for screening to identify additional MRP1 inhibitors.
US20090176836 3-{[(3-amino-3-benzyltetrahydrofuran-2-yl)oxy]methyl}-N-[(1R)-1-(4-fluorophenyl)ethyl]-5-[(methylsulfonyl)(propyl)amino]benzamide, used for preventing the formation of insoluble amyloid proteins The present invention is directed to cyclic ketal compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
EP2721025A1 New selective ccr2 antagonists The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain.
CN103284952A Medical composition containing fenofibrate The invention discloses fenofibrate compound powder which is prepared by an anti-solvent method. Fenofibrate is accelerated to be dissolved out, so that the deficiency that fenofibrate is hardly soluble in water and the bioavailability is low is solved. Meanwhile, the invention further provides a medical composition containing fenofibrate and a preparation method thereof. The method overcomes difficulty in the preparation production process due to great viscidity of the fenofibrate compound powder, so that the contents of main medicines are good in uniformity. Powder in the pelletization process is prevented from rising, the loss of main medicines is reduced, and the mobility of medicine particles is improved, so that the medical composition is suitable for industrialized production in a large scale.
WO2009053553A1 Rimonabant 2-methoxyethanol solvate and method for preparing same The invention relates to a rimonabant 2-methoxyethanol solvate, and to a method for preparing the same.
WO2013087578A1 Disubstituted benzothienyl-pyrrolotriazines and their use as fgfr kinase inhibitors This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group -CH2-OR3, -CH2-NR4R5 or -C(=0)- NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group - CR8AR8B-OH, -CH2-NR9R10, -C(=0)-NR11R12 or -CH2-OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
WO2006083618A1 NANDROLONE 17ß-CARBONATES Disclosed are compounds of the formula (I) wherein R is C1-C30 alkyl, which may be optionally further substituted with one or more C5-C8 cycloalkyl groups, or a C5-C12 cycloalkyl, which may be optionally substituted with one or more C1-C30 alkyl groups, R’ is hydrogen or lower alkyl, R” is a C1-C30 alkyl or halo, and the bond between C14 and C15 can be a single bond or double bond. Also disclosed are pharmaceutical compositions comprising such compounds and methods of use thereof. These compounds can find use in treating a number of diseases or conditions such as hypogonadism, hypergonadism, osteoporosis, and anemia, in providing hormonal therapy and contraception, as an anabolic agent, and in suppressing the release of hormones such as the luteinizing hormone.
CN1939269A Oral preparation containing ampicillin and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains ampicillin. Its preparing process is also disclosed.
US6936714 Compounds of the saframycin-ecteinascidin series, uses, and synthesis thereof Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: wherein R1 and R4 is H, a C1 to C4 alkyl group, or an acyl group; wherein R2 is an ether, ester, amide, or a phthalimide group; wherein R3 is ═O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R5 is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R6 is ═O, OH, OCH3, CN, or an acyloxy group; wherein R7, is ═O, OH, halogen, an ether group, or an acyl group; wherein R8 and R9 are independently H, CH3, OCH3, OC2H5, CF3, halogen such as Br and F, or R8 and R9 are joined together as a methylenedioxy group, or other five or six membered ring; wherein R10 and R11 are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; wherein R12 is H, a C1 to C4 alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.
US20080275112 3-Aminoadamantane-1-carboxylic acid derivatives in which position 5 or 7 of the adamantane skeleton has been optionally substituted; coupling of monomeric amino acid derivatives to oligomers; antiviral agents GABA analogues, oligopeptides, ion channel modulators, and peptidic catalysts The present invention describes 1-aminoadamantane derivatives and 3-aminoadamantane-1-carboxylic derivatives in which the 5- or 7-position of the basic adamantane structure can be optionally substituted, methods for the production of the compounds based on the present invention, and methods for the coupling of the monomeric 3-aminoadamantane-1-carboxylic derivatives thus obtained to oligomers. The compounds based on the present invention are suitable for the utilisation as antiviral active ingredients, artificial ion channels, as well as for the therapy, diagnostics and prophylaxis of diseases in which a dysfunction of the GABA system occurs.
US7291608 Anti-inflammatory 17.β.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.α There are provided compounds of formula (I) wherein the variables are as defined by the present specification; and solvates thereof, processes for preparing them and their use in therapy.
US20090253775 Compositions and Methods for Therapy and Diagnosis of Cancer and Cancer Metastasis The present invention relates to methods which make possible to assess and/or prognose a cancer disease, the metastatic behaviour of a cancer disease and/or the occurrence of a relapse of cancer. In particular, the methods of the invention make possible to assess and/or prognose the occurrence of cancer metastasis, in particular distant metastasis. Preferably, the methods of the invention allow to discriminate malign from benign conditions.
CN101048381A Novel imidazolidine derivative and use thereof According to the present invention, a compound represented by formula (I): wherein Q is: A is a hydrogen atom, a halogen atom, -ORa or a C 1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a C 1-6 alkyl group; m is selected from integers from 0 to 3; R 2 and R 3 are independently selected from a C 1-6 alkyl group; X 1 and X 2 are independently selected from O and S; Y is selected from an arylene group and a divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group, wherein the arylene group and the heterocyclic group may be substituted by 1 to 3 substituents independently selected from E 1 ; E 1 is independently selected from a hydroxyl group, a halogen atom, a C 1-4 alkyl group, a cyano group, a C 1-4 alkoxy group, a carbamoyl group, a C 1-4 alkylcarbamoyl group, a di(C 1-4 alkyl)carbamoyl group, an amino group, a C 1-4 alkylamino group, a di(C 1-4 alkyl)amino group, a sulfamoyl group, a C 1-4 alkylsulfamoyl group and a di(C 1-4 alkyl)sulfamoyl group; Z is -CON(-Ra)-, -CO-, -COO-, -NRa-C(=NH)NRb-, -NRa-C(=N-CN)NRb-, N(-Ra)COO-, -C(=NH)-, -SO 2 -, -SO 2 N(-Ra)-, -SO 2 NR 1 -, -N(-Ra)CO-, -N(-Ra)CON(-Rb)-, -N(COR 1 )CO-, -N(-Ra)SO 2 -, -N(SO 2 R 1 )SO2-, -N(-Ra)- or -N(-Ra)SO 2 N(-Rb)-; R 1 is independently a hydrogen atom, a hydroxyl group, a C 1-6 alkyl group which may be substituted by one or more substituents, a heterocyclic group which may be substituted by one or more substituents, an aryl group which may be substituted by one or more substituents, a C 3-8 cycloalkyl group which may be substituted by one or more substituents or a C 3-8 cycloalkenyl group which may be substituted by one or more substituents, or a salt, prodrug or solvate thereof is provided. Furthermore, a pharmaceutical composition containing the compound, and the like are also provided.
CN1568991A Desloratadine diapersible tablet and its preparation method The invention relates to desloratadine diapersible tablet and its preparation method, which comprises desloratadine diapersible, dressing material, adsorbent, crumbling agent, bulking agent, water-soluble excipient, perfume compound, sweetener, and lubricating agent.
CN101234951A Biphenyls compound and its preparation method and application A biphenyl compound and a preparation method and application thereof are disclosed. The invention provides a biphenyl compound which has excellent biological activity, oxidation resistance and cancer-cell inhibition ability, and also provides a preparation method and application thereof. The biphenyl compound is a colorless acicular crystal obtained from secondary metabolite of fungus growing in mangroves and has biological activity, oxidation resistance property and cancer-cell inhibition ability. The preparation method comprises preparation of seed liquid and fermentation liquid of Aspergillus clavatonanicus BYY-1 and extraction and refinement of the biphenyl compound. The biphenyl compound has considerably outstanding anti-tumor and anti-oxidation function and can be used for preparation of anti-tumor drugs and applied to the fields of medicine, cosmetics and food as an antioxidant.
US20080221200 Dipeptidyl-peptidase (DPP) IV inhibitor N-peptidyl-O-aroyl hydroxylamine and immunosuppressor or immunomodulator; autoimmune diseases, graft rejection; antidiabetic agents; Alzheimer's, Parkinson's disease; obesity, retinopathy, nephropathy, neuropathy, schizophrenia; cognition activators The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and comprising at least one immunosuppressive or immunomodulator agent, or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention, delay of progression or treatment of diseases and disorders that may be inhibited by DPP IV inhibition, for the prevention, delay of progression or treatment of autoimmune diseases, and the disorders associated therewith, or for the prevention, delay of progression or treatment of graft rejection.
CN1602851A Dripping pills of benactyzine hydrochloride and its preparation The invention uses super micro shattering and benactyzine drop pills producing the technology to produce fenfluramine drop pills, reaching the purposes such as increasing speed, and dissolution of disintegration, increasing the medicine stability, reducing the dose of auxiliary materials and decreasing cost, with rapid effect and convenient use. It can be buccal as well as deglutition, has remarkable conformity, and is especially suitable for children, older man, sicker in bed or with difficulty of swallowing.
US7342019 5, 6-diaryl-pyrazine-2-amide derivatives as CB1 antagonists The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R1 and R2 independently represent: a C1-6alkyl group; an optionally substituted (amino)C1-4alkyl-group; an optionally substituted non-aromatic C3-15carbocyclic group; a (C3-12cycloalkyl)C1-3alkyl-group; a group —(CH2)r(phenyl)s in which r is 0, 1, 2, 3 or 4, s is 1 when r is 0 otherwise s is 1 or 2 and the phenyl groups are optionally independently substituted by Z; naphthyl; anthracenyl; an optionally substituted saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen; 1-adamantylmethyl; a group —(CH2)t Het in which t is 0, 1, 2, 3 or 4, and the alkylene chain is optionally substituted and Het represents an optionally substituted aromatic heterocycle; or R1 represents H and R2 is as defined above; or R1 and R2 together with the nitrogen atom to which they are attached represent a saturated optionally substituted 5 to 8 membered heterocyclic group as defined above; X is CO or SO2; Y is absent or represents NH optionally substitututed by a C1-3alkyl group; R3 and R4 independently represent phenyl, thienyl or pyridyl substituted by Z; Z represents a C1-3alkyl group, a C1-3alkoxy group, hydroxy, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, trifluoromethylsulphonyl, nitro, amino, mono or di C1-3alkylamino, mono or di C1-3alkylamido, C1-3alkylsulphonyl, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkyl carbamoyl, sulphamoyl and acetyl; and R5 is H, a C1-3alkyl group, a C1-3alkoxymethyl group, trifluoromethyl, a hydroxyC1-3alkyl group, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula —CONHNRaRb; with the provisos; and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
CN101271089B Method for identifying allantoin in Cistanche plant variety An application of allantoin in the variety identification of a desertliving cistanche plant and a new usage for lowering the blood lipid use the absorption and separation technology of macroporous absorption resin and granular activated carbon to obtain the allantoin and components containing the allantoin from the desertliving cistanche by extraction and separation, and the chemical structure thereof is determined by analyzing the physical and chemical data and the spectral data. The allantoin is the component which is firstly discovered in the desertliving cistanche plant, as cistanche tubulosa does not contain the component, the allantoin can be used for identifying the characteristic of the cistanche tubulosa and other desertliving cistanches; adopting the yeast double-hybrid system test of the molecular biology simultaneously, the new medical usage of the allantoin for lowering the blood lipid is determined.
WO2007020478A1 Virucidal solutions The present invention relates to improved virucidal agents, and particularly to virucidal solutions, for killing harmful viruses such those causing avian viral diseases.
CN103347535A Liquid viral formulations Provided herein are liquid viral formulations useful for the stabilization and storage of viruses and methods of preparing these formulations. The liquid viral formulations described herein include a virus (e.g., a purified virus) and a non-viral composition including excipients and a liquid carrier. The formulations can be used, for example, to retain the infectivity or immunogenicity of viruses during periods of storage.
CN101597572A Oxytropis ehrig sporangium FEL6-AS2 for synthesizing SW and application thereof The invention discloses an oxytropis ehrig sporangium FEL6-AS2 for synthesizing SW, which is preserved in the China Center for Type Culture Collection on October 8, 2008, with the preservation serial number of CCTCC No: M 208145. The colony of the strain is circular and is white originally, the color is gradually changed into a grey-white color, a grey-black color and a black color along with the prolongation of the culture time, and the center protrudes. The mycelium has transverse septa and does not have longitudinal septa, part of aged hyphae puts forth conidium peduncles, and the conidium peduncles have branches. Conidia and the conidium peduncles have the transverse septa and do not have the longitudinal septa, the transverse septa of the conidia are thicker, the number of the transverse septa is 1 to 4, sporules are in bar shapes and are approximately cylindrical, parts of the sporules are circular, and the size of the conidia is 20 to 80mum*6 to 12mum; and the strain is obtained from the leaves, stems and seeds of astragalus root with straight stems by artificial separation and screening, and has the function of synthesizing the SW which is the main toxin of locoweed.
US7029672 Use of quinone Q10 for the treatment of ocular diseases The present invention relates to the use of Coenzyme Q10 or functionally equivalent derivatives thereof, through topical or systemic administration, for the prevention, the treatment and/or attenuation of degenerative ocular pathologies, said pathologies being of an heredofamilial, inflammatory, dysmetabolic, senile age-related nature, the degenerative process deriving from apoptotic events caused by hypoxia or other detrimental stimuli due to ischemia or to the lack of trophic factors.
CN1985822A Enteric omeprazole micropill and its preparing method The present invention discloses a kind of enteric omeprazole micropill preparation and its preparation process. The enteric omeprazole micropill preparation has core of omeprazole or its single antimer subsalt as the active component and excipient and middle isolating coating and enteric protecting layer to coat the core. The enteric omeprazole micropill preparation is prepared directly with the main medicine component and supplementary materials including magnesia as the stabilizer, hydroxypropylmethyl cellulose and talcum powder.
CN101084883A Capsaicin percutaneous controlled-release paster and preparation method The invention discloses a capsaicin transdermal controlled release patch and its preparation method. the method comprises mixing capsaicin 0.05-2%, hydrophilic pressure sensitive adhesive substrate 78-98% and compound transdermal accelerant 1.0-20%, preparing into solid disperse substance, extrusion coating on subbottom paper, drying at 50deg.C, backing with PVC or non-woven fabrics for recombination of material, and blanking into pieces with certain size and specification to obtain final product. The invention has the advantages of definite product effective component, low dose, high standardization degree, few adjuvant, simple production technology, and stable and controlable product quality.
CN101095462A Method for synthesizing the feed additive - isoflavone The invention discloses a method for preparing a kind of feedstuff addictive--isoflavone, which comprises following steps: preparing phenylbenzylketone with substituted-4 resorcin and substituted-4 resorcinphenylacetyl, carrying out ring closure reaction with waterless carboxylate and relevant anhydride, getting isoflavone with substitution group at second position. The invention is characterized by non use of special device, temperate reaction condition, easy operation, high productivity and easy for industrial production. The invention is also characterized in that: (1)it employs resorcinphenylacetyl to replace acetate and benzene cyanogen, which widens the reaction selectivity; (2)employing waterless carboxylate and relevant anhydride and benzyl ketone to carry out ring closure reaction, to replace C1 solvent and potential C1 solvent; (3)the isoflavone contains substituted group.
US7399745 polypeptides, fragments and/or variants, used for treatment of metabolic disorders, such as diabetes and obesity; hypoglycemic agents The invention provides polypeptides that act both as an agonist of the GLP-1 receptor and an antagonist of the glucagon receptor. Such polypeptides are useful for treating individuals with type 2 diabetes or other metabolic disorders.
WO2006117657A1 Triazolone derivatives as anti-inflammatory agents The present invention relates to novel triazolone derivatives as anti-inflammatory agents. The compounds described herein can be useful for inhibition and prevention of inflammation and associated pathologies including inflammatory and autoimmune diseases such as sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis. This invention also relates to pharmacological compositions containing compounds described herein and the methods of treating sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis, and other inflammatory and/or autoimmune disorders, using the compounds.
CN102895177A Metronidazole mucilage and preparation method thereof The invention discloses a metronidazole mucilage which is characterized by comprising the following components in parts by weight: 1000 parts of water, 1-10 parts of metronidazole, 10-300 parts of glycerol and/or propylene glycol, 0.1-10 parts of chlorhexidine, 1-100 parts of polyethylene oxide, 5-100 parts of polyoxyethylene polypropylene oxide copolymer and 0.05-0.5 parts of EDTA (Ethylene Diamine Tetraacetic Acid) disodium. The invention also discloses a preparation method of the metronidazole mucilage, comprising the steps of dissolving metronidazole by using water, adding other components, and fully and uniformly mixing to form a colloidal solution. The metronidazole mucilage disclosed by the invention has the due efficacy of metronidazole drugs and is capable of simulating cervix uteri, vagina mucus and moist local ecological environment of healthy women, suitable for the treatment and the rehabilitation protection of female reproductive tract infections, menopause vaginitis and reproductive tract infection after the uterus ovarian surgery and capable of overcoming the defect that the dispersion of traditional vaginal effervescent tablets, vaginal suppositories and lotions may be influenced due to insufficient environmental moisture.
US7576115 1-methyl,3-alkaminothiocarbonylhydrazonomethyl,4-hydroxy,5-phenyl pyrazole; low-molecular-weight, nonpeptidic thrombopoietin receptor agonist; oral administration; bioavailability; blood disorders; platelet-increasing agents; angiogenesis; arteriosclerosis; blood/stem cell stimulant; thrombocytopenia A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or is pharmaceutically acceptable salt of the compound or a solvate thereof.
WO2014086316A1 Substituted pyridopyrazines as syk inhibitors The present invention relates to pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, L, m, p and W are as defined in the specification.
CN101601658A Method for preparing valnemulin hydrochloride coating granule The invention belongs to a process for preparing a valnemulin hydrochloride premix of pleuromutilin antibiotics specially used for animals, and in particular relates to a method for preparing a valnemulin hydrochloride coating granule. The method comprises the following process steps of pre-granulation of the valnemulin hydrochloride, preparation of coating solution, coating of the valnemulin hydrochloride and the like. The method has the advantages of solving the problems existing in the prior art that the valnemulin hydrochloride materials are hygroscopic, sensitive to light and strong in powder irritation, and are easily decomposed when being mixed with feed and the like, effectively achieving the aim of odor masking and the like; moreover, after coating, the coating granule is stable under conditions of a light accelerating experiment.
US7297688 An oral contraceptive starter kit comprising at least two cycle packs of oral contraceptives containing an estrogen and a progestin, and having penultimate cycle with greater steroid dosage than last cycle pack dosage The present invention provides a contraceptive kit which helps to overcome or ameliorate the problem of breakthrough bleeding and spotting associated with lowest dose (15-20 ug EE) estrogen contraceptives.
CN103417491A Memantine hydrochloride slow-release pellet preparation and preparation method thereof The invention relates to a memantine hydrochloride slow-release pellet preparation and a preparation method thereof. The memantine hydrochloride slow-release pellet preparation comprises a blank pellet core as a nuclear parent and memantine hydrochloride medicine slow-release composite layer wrapped as an outer layer. The preparation is characterized in that the blank pellet core and the memantine hydrochloride medicine slow-release composite layer are in the weight ratio of 2-6:1; the memantine hydrochloride medicine slow-release composite layer contains 10-40% of memantine hydrochloride, 50-70% of a slow-release material and 0.1-20% of other accessories. The slow-release pellet prepared by the invention has high roundness and good fluidity, can obtain high yield during wrapping of medicine and the slow release material, and has good reappearance. The simple preparation technology of the slow-release pellet is not restrained by place or equipment and suitable for industrialized production.
US20090170793 Theophylline-dependent riboswitches which modulate RNA splicing; made by insertion of a high affinity theophylline binding aptamer into the 3' splice site region, 5' splice site region, or branchpoint sequence (BPS) of a pre-mRNA modulates RNA splicing in the presence of theophylline The present invention relates to riboswitches that have been engineered to regulate pre-mRNA splicing. In particular, the insertion of a high affinity theophylline binding aptamer into the 3′ splice site region, 5′ splice site region, or branchpoint sequence (BPS) of a pre-mRNA modulates RNA splicing in the presence of theophylline. Accordingly, the aspects of the present invention include, but are not limited to, theophylline-dependent riboswitches which modulate RNA splicing, methods of modulating RNA splicing using theophylline and its corresponding riboswitches, methods of improving/identifying theophylline-dependent riboswitches, methods of treating diseases associated with or caused by abnormal RNA splicing.
CN1988896A Use of compounds active on the sigma receptor for the treatment of mechanical allodynia The present invention refert to the use of compounds active on the sigma receptor for the treatment of mechanical allodynia.
US20090181060 Skin-care compositions In certain embodiments provided are composition suitable for cleansing or treating the skin, the composition comprising: (i) at least 90% water; (ii) a non-ionic surfactant; (iii) one or more hydrophobic emollients present in a concentration from about 200 parts per million (ppm) to about 4000 ppm, and wherein the composition has a ratio of total surfactant concentration to total hydrophobic emollient concentration that is from about 0.5 to about 2.5. In other embodiments, provided are articles comprising a water-insoluble absorbent substrate and a composition comprising a polyol polyhydroxystearate or a water-soluble glyceryl polyacrylate impregnated therein.
CN102247573A Medicinal injection for treating delirium The invention relates to a medicinal injection for treating delirium and a preparation method thereof, and relates to application of poloxamer to the preparation of refreshment calming injections. The medicinal injection is processed by using 7.5 parts of musk, 30 parts of turmeric root-tuber, 1 part of borneol, 30 parts of bupleurum, gardenia and 1 to 200 parts of poloxamer serving as a solubilizer.
CN102973623A Separation method of ginseng rare saponins in ginseng fibrils The invention belongs to a method for separating ginseng rare saponins in ginseng fibrils. The method comprises the following steps of: taking fresh ginseng fibrils as raw materials; steaming and machining at a certain temperature; after crushing, heating and reflowing through ethanol with the concentration of 80% to obtain the ginseng rare total saponins; separating and purifying by macro-porous resin and collecting an eluting component of the ethanol with the concentration of 80%; then utilizing methanol to dissolve the eluting component of the ethanol with the concentration of 80% by utilizing the characteristics that the polarity of the rare saponins is small and the solubility difference exits in different solvents; and adding acetone to precipitate to further purify the obtained component to obtain the ginseng rare saponins with the stable component. Through RRLC-Q-TOF-MS detection analysis, the ginseng rare saponins comprise 20(S/R)-Rh1, Rg9, Rg8, F2, Rg6, Rg4, Rk3, Rh4, 20(S/R)-Rg3, 20(S/R)-Rs3, Rk1, Rg5, 20(S/R)-Rh2, Rs5, Rs4, Rk2 and Rh3. The method is low in cost, is simple and fast, is efficient and is easy to operate.
EP2525794A1 5-(1h-pyrazol-5-yl)thiazole-based compounds for the treatment of diseases and disorders of the eye Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use. Particular compounds are of the formula (I)
CN102671024A Ointment for treating oral ulcer and preparation method thereof The invention discloses an ointment for treating oral ulcer and a preparation method thereof. The ointment is characterized by being prepared from the following raw medicines in parts by weight: 8-12 parts of citronella, 8-12 parts of spiranthes sinensis ames, 8-12 parts of euonymus alatus, 8-12 parts of erigeron breviscapus, 8-12 parts of colophony powder, 4-6 parts of purslane, 1 part of ophicalcitum and 14-20 parts of tea oil. The preparation method comprises the steps of: extracting volatile oil from the citronella and the erigeron breviscapus, decocting the spiranthes sinensis ames, the euonymus alatus and the purslane with water, concentrating the filtrate, drying, smashing, adding the tea oil at a temperature of 200-220 DEG C, adding the colophony powder and the ophicalcitum powderafter filtering the oil, decocting till the drip is shaped like a bead, spraying cold water to remove water toxin, cooling to the normal temperature, adding the volatile oil, and uniformly stirring to obtain the ointment. Proven by clinical experiments, the ointment has the advantages of capability of shortening the healing time and relieving the postoperative pain, reliability in curative effectand safety in use when being used for treating the oral ulcer.
US8088910 Isolated multiple sclerosis (MS)-associated retrovirus (MSRV) nucleic acids corresponding to the gag region An isolated polynucleotide having a nucleotide sequence selected from the group consisting of (a) SEQ ID NO: 21, (b) the full-length sequences encoding a polypeptide having a peptide sequence selected from the group consisting of SEQ ID NOs: 25 and 26, and (c) the full-length complementary sequences to the sequences set forth in (a) or (b).
CN103316006A Application of Myriberine A in preparation of medicine for treating lung cancer The invention discloses an application of Myriberine A in the preparation of a medicine for treating lung cancer. The compound shows a good anti-lung cancer activity, can be used in the preparation of an anti-lung cancer medicine, and belongs to the technical field of new application of medicines. Myriberine A can remarkably inhibit in vitro cultured non-small cell lung cancer cell A549, maxicell lung cancer cell NCI-H460, lung squamous carcinoma cell HTB-8 and human lung squamous cell carcinoma cell QG-5, has little effect of inhibiting human normal hepatocyte LO2 and peripheral blood lymphocyte, and shows obvious selectivity. The application of Myriberine A in the preparation of a medicine for treating lung cancer is disclosed for the first time. The matrix type belongs to a brand new matrix type, and Myriberine A has an unexpectedly strong activity of inhibiting the lung carcinoma cell.
CN101297973A Highly bioadhesive and thermosensitive hydrogel, and preparation method and application thereof The invention relates to a temperature sensitive hydrogel with high bioadhesion, the components of which includes: 10 percent to 40 percent of poloxamer, 0.1 percent to 10 percent of carboxymethyl chitosan and 50 percent to 99.8 percent of water while the percentages are weight percentages. The invention also provides a preparation method of the temperature sensitive hydrogel: the poloxamer is added with water to be evenly stirred, and added with the carboxymethyl chitosan to be evenly stirred to obtain the temperature sensitive hydrogel with high bioadhesion. The temperature sensitive hydrogel can be used as a drug carrier after being defoamed. The preparation method of the invention can be used for the preparation of mucosal drug delivery preparations and injection drug delivery preparations and obtain an intelligent drug slow-release preparation, the hydrogel property of which meets the application requirements in the conditions of pathological mechanism and physiology, thus being convenient for clinical application, being capable of reducing the frequency of the drug delivery and improving the adaptability of patients; enhancing treatment effect and reducing toxic and side effects. Compared with the pure poloxamer hydrogel, the temperature sensitive hydrogel of the invention can obviously enhance the mechanical strength and the mucosa bioadhesion and obviously prolong the detention time in vivo under the condition of ensuring excellent fluidity and favorable hydrogel temperature condition.
US6872707 Prevention, therapy of bacteria infections The invention relates to halo derivatives of 9a-N-(N′-arylcarbamoyl)- and 9a-N-(N′-arylthiocarbamoyl)-9-deoxo-9a-aza-9a-homoerythromycin A of the general formula (I) wherein R has the meaning of a substituted aryl group of the formula (II) wherein substituents a, b, c, d and e are the same or different and at least one of them has the meaning of halo, a (C1-C6)haloalkyl or a (C1-C6)haloalkoxy group, whereas the remaining ones have the meaning of hydrogen, halo, a (C1-C6)alkyl or a (C1-C6)alkoxy group, and X has the meaning of oxygen or sulfur, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to a process for their preparation, to a process for the preparation of pharmaceutical compositions comprising them and to the use of these pharmaceutical compositions for the treatment or prevention of bacterial infections.
US6921825 Pyrazolo-triazolo- pyrimidine, triazolo-triazolo-pyrimidine and imidazolo-triazolo-pyrimidine derivatives useful for the treatment of hypertension, inflammation, mast cell degranulation, cardiac hypoxia, and ischemia The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.
US8075903 Dengue tetravalent vaccine containing a common 30 nucleotide deletion in the 3′-UTR of dengue types 1, 2, 3, and 4 or antigenic chimeric dengue viruses 1, 2, 3, and 4 The invention relates to a dengue virus tetravalent vaccine containing a common 30 nucleotide deletion (Δ30) in the 3′-untranslated region of the genome of dengue virus serotypes 1, 2, 3, and 4, or antigenic chimeric dengue viruses of serotypes 1, 2, 3, and 4.
CN102659617A L-tyrosine derivative, medicine compound and application thereof The invention discloses a compound with a formula I structure, especially a medicine compound which is composed of the compound with the formula I structure as active principle and one or more pharmaceutically acceptable carrier, excipient or diluent. The compound with the formula I structure provided by the invention is mainly used for treating tumor diseases and especially has an activity for restraining tumor metastasis, so that the compound can be used for preparing the medicine for restraining liver cancer metastasis.
CN103263413A Ketorolac implant and preparation method thereof The invention provides a ketorolac implant and a preparation method thereof. The implant which contains ketorolac and a degradable carrier is prepared by using a hot melt extrusion method, can release drugs in a zero-level dynamic way within a preset drug release time and can be used for preventing or treating acute or chronic pain and inflammation. The ketorolac implant prepared by the invention is stable in release and free of burst release effect and has great advantages in clinic application.
CN102793714A Application of mecobalamine and analogue to protein tyrosine phosphatases SHP-1 inhibitor The invention belongs to the technical field of a tyrosine phosphatase inhibitor and particularly relates to the application of mecobalamine and analogue to a protein tyrosine phosphatases SHP-1 inhibitor. Experiments show that the mecobalamine has IC50 of 20.0muM on tyrosine phosphatases SHP-1 and has the inhibition constant Ki of 179.7muM on the tyrosine phosphatases SHP-1; as the tyrosine phosphatases SHP-1 inhibitor, the mecobalamine obviously improves the phosphorylation level of an insulin receptor IR in an insulin signal pathway; and with the rising of the concentration of the mecobalamine, the phosphorylation level of the insulin receptor IR is obviously improved. The mecobalamine is further used for preparing food, a medicament or a food and medicinal composition for treating and preventing diseases related to the overhigh or overexpressed activity of the protein tyrosine phosphatases SHP-1.
US6908942 Carbocyclic oxy amines such as 2,2-dimethyl-3-(4-fluorobenzyl) ether-4-methoxy-6-(4-methoxybenzyl)amino Benzopyran and libraries, used for prophylaxis of eating disorders induced by lipid peroxidation; antioxidants The present invention provides (i) 6-amino-2,2-dimethyl-3,4,6-trisubstituted benzopyran derivatives; (ii) a process for synthesizing benzopyran derivatives with high efficiency by parallel synthesis on a solid-phase as one of combinatorial chemical synthesis technologies; and (iii) a use of the benzopyran derivatives for preventing and treating diseases or disorders induced by promotion of lipid peroxidation or accumulation of oxidized products.
CN102233093A Qingsanghoubao The invention discloses a qingsanghoubao which comprises the following raw material herbs by weight: 1 part of dark plum, 2 parts of honeysuckle, 3 parts of scutellaria, 4 parts of isatis roots, 1 part of rheum officinale, 2 parts of borneol, 2 parts of sterculia lychnophora, 1 part of balloonflower roots, 2 parts of Zhejiang fritillaria, 2 parts of grosvenor momordica, 3 parts of radix scrophulariae, 2 parts of tuber of dwarf lilyturf, 1 part of tenninlia chebula, 3 parts of licorice, 1 part of eucalyptus oil, 1 part of menthol, and 5 parts of cane sugar. The invention has the functions of clearing pharynx, moistening throat, and health care. The invention not only has antiphlogistic and analgesic effect, but also can generate body fluid and moisten throat, and has good curative effect on pharynx and throat diseases of pharyngeal dryness, edema, pain with hoarseness.
CN101716256B Preparation used for strengthening immunity The invention discloses a preparation used for strengthening immunity and inhibiting tumor. The preparation is characterized by being prepared from following raw materials by weight proportion: 290-350g bat moth paecilomyces powder, 72-84g medlar extract, and 1-5g taurine; and the preparation can be prepared by the steps of: after processes of enzymolysis extraction and the like, superfine grinding and mixing to obtain fine powder, and combining with pharmaceutical excipients to make into capsules, tablets, granules and the like. The invention has the advantages that, through all actions of the bat moth paecilomyces powder, the taurine and the medlar extract, immune cells are activated and immunity function of all organic tissues and systems is enhanced, thereby achieving the effects of improving organism immunity function and enhancing resistibility; and meanwhile, the preparation can inhibit tumor growth and kill tumor cells and has a favorable anti-tumor effect. The invention is suitable for curing various infections caused by week immunity and other diseases and for convalescents after tumor operations.
US20090017107 Novel composition to increase libido The present invention relates to a composition for increasing testosterone physiological levels comprising a sufficient amount of at least two ketosteroid derivatives of testosterone metabolism in association with a liposomal carrier bound to a saliva-absorbing carrier, wherein said increase in testosterone levels increases libido.
US20110039928 Cetylated fatty acid and alkali buffered creatine anti-inflammatory composition An anti-inflammatory composition for treatment of inflamed joints. This composition includes an alkali buffered creatine and a cetylated fatty acid. The composition can be used for treating inflammation either by oral ingestion or by topical treatment.
US20110294862 Treatment or prevention of hypotension and shock A method for the prevention and treatment of hypotension and shock due to low peripheral resistance, comprising administering to a mammal in need thereof an effective amount of a certain imidazole derivative or pharmaceutically acceptable ester or salt thereof, and a method for the treatment of cardiopulmonary resuscitation, comprising administering to a mammal in need thereof an effective amount of a certain imidazole derivative or pharmaceutically acceptable ester or salt thereof.
EP1534281A1 N-sulfonylpiperidines as metalloproteinase inhibitors (tace) Compounds of formula (1), wherein Z is -CONR15OH or -N(OH)CHO and X is -(CR9R10)t-Q-(CR11R12)u- (where t and u are independently 0 or 1 with the proviso that t and u cannot both be 0);are inhibitors of metalloproteinases and in particular TACE.
US7875603 phenyl-, pyridyl-, pyrimidyl- and purine- derivatives; anticarcinogenic agent; solid tumor: breast, colorectal, lung, prostate, and ovarian The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.
CN1559431A Disperse tablet contg. klinemycin hydrochloride palmitate, and its prepn. method A dispersing tablet of clindamycin hydrochloride palmitate and its preparing process are disclosed.
CN101264074B Oxybuprocaine gel and preparation thereof The invention discloses a surface anesthesia drug, in particular to a gel preparation using oxybuprocaine as main component and the preparation method, which is prepared by following raw material according to weight account: oxybuprocaine 1 to 5, benzalkonium bromide 0.05 to 0.15, disodium edta 0.05 to 0.15, methyl cellulose 12 to 22. The gel preparation using oxybuprocaine as main component has the advantages of fast efficacy, strong infiltration, quick absorption, long action time and small poison and side effect through experiment showing.
CA2127193C 2-[1-(1,3-thiazolin-2-yl)azetidin-3-yl] thio-carbapenem derivatives Novel carbapenem compounds, (1R,5S,6S)-2-[1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio-6-[(R)-1-hydroxy-ethyl]-1-methyl-carbapen-2-em-3-carboxyic acid derivatives. These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a [1-(1,3-thiazolin -2-yl)azetidin-3-yl]thio group introduced at the 2-position.(see formula I) In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group;group -COOR1 (R1 is hydrogen or lower alkyl group); or group -CONR2R3 (R2 and R3 are, independently each other, hydrogen or lower alkyl), and Y is carboxy, -COO~ or protected carboxy. These compounds are useful antibiotics for prevention and treatment of bacterial infections.
WO2007148158A1 Enantiomerically pure flavone derivatives for the treatment of poliferative disorders and processes for their preparation The present invention relates to an enantiomerically pure (+)-trans-enantiomer of a compound represented by the following formula (I): wherein R1, R2, R3, R4 and R9 are as defined in the specification; enantiomerically pure intermediates thereof, to processes for the preparation of the enantiomerically pure compound and its intermediates, and to a pharmaceutical composition comprising the enantiomerically pure compound. The compound of formula (I) is useful for the treatment of diseases or disorders mediated by the inhibition of cyclin dependant kinase, such as cancer.
EP1582210A2 Compositions and methods for treating or preventing surgical adhesions The present invention provides methods for treating or preventing surgical adhesions comprising the step of delivering to the site of inflammation an anti-microtubule agent,or analogue or derivative thereof.
US20120328672 Composition and method of separating bentonite into particles having discrete size and density ranges capable of binding biological toxins and chemotherapeutic agents. A low heavy metal (i.e. cadmium, mercury) containing calcium aluminum silicate product produced by the method of Air Classification. The method comprises using an air classification system for separating a cadmium containing calcium aluminum silicate feed stock into at least a first fraction and a second fraction. The first separation fraction contains material having an average particle size over 100 um, and the second fraction contains material having an average particle size under 100 um.
US20120302595 Fkbp52-tau interaction as a novel therapeutical target for treating the neurological disorders involving tau dysfunction The invention relates generally to neuro-protection and repair in neurological disorders involving Tau dysfunction (including Alzheimer's disease). The invention describes AND INCLUDES a direct interaction between proteins FKBP52 and Tau. More particularly, the invention relates to a method for screening a drug for the prevention and treatment of neurological disorders involving Tau dysfunction comprising the following steps: a) determining the ability of a candidate compound, to modulate the interaction between a Tau polypeptide and a FKBP52 polypeptide and b) selecting positively the candidate compound that modulates said interaction. The present invention finally relates to diagnostic, prognostic, and monitoring assays of neurological disorders involving Tau dysfunction.
EP1580192A2 16-Hydroxyestratrienes as selective estrogens 3,16-Dihydroxy-1,3,5(10)-estratriene derivatives (I) are new. - 3,16-Dihydroxy-1,3,5(10)-estratriene derivatives of formula (I) are new: - thick black line in ring = single or double bond; - R1 = H, halo, OH, Me, CF3, OMe or OEt; - R2 = H, halo, OH or 1-6C optionally saturated alkoxy; - R4 = H, halo, 1-10C optionally saturated alkyl, CF3, C2F5 or 1-6C optionally saturated alkoxy; - R7 = H, halo, 1-10C optionally saturated alkyl (optionally fully or partly fluorinated), 1-6C optionally saturated alkoxy or optionally substituted aryl or heteroaryl; - R8 = H, , 1-10C optionally saturated alkyl (optionally fully or partly fluorinated) or CN; - R9 = H, Me, Et, CF3 or C2F5; - R11 = H, ONO2, OH, SH, halo, CH2Cl, 1-10C optionally saturated alkyl (optionally fully or partly fluorinated), 1-6C optionally saturated alkoxy, 1-6C optionally saturated alkylthio or optionally substituted aryl or heteroaryl; - R13 = Me, Et, CF3 or C2F5; - R14 = H or 1-10C optionally saturated alkyl (optionally fully or partly fluorinated); - R15 = H, halo or 1-10C optionally saturated alkyl (optionally fully or partly fluorinated and optionally interrupted by O, S, SO, SO2 or NR15'); - R15' = H or 1-3C alkyl; - R16 = optionally saturated 1-10C alkyl (optionally partly or fully fluorinated), CF3, or pentafluoroethyl, CN or H ; - R17 = H, OH, halo or 1-10C optionally saturated alkyl (optionally fully or partly fluorinated); or - R14+R15 = optionally mono- or dihalogenated methylene; - wavy lines = alpha or beta configuration. - Excluded are: - 1,3,5(10)-estratriene-3,16 alpha -diol (Ia); - 1,3,5(10)-estratriene-3,16 beta -diol (Ib); - 1,3,5(10),7-estratetraene-3,16 alpha -diol (Ic); and - 1,3,5(10),7-estratetraene-3,16 beta -diol (Id). - Independent claims are also included for the following: - (1) use of compounds (I), including (Ia)-(Id), for treating diseases caused by estrogen deficiency in women and men; - (2) use of the partial structure of formula (II) as a component of the total structure of compounds exhibiting a dissociation in estrogenic activity in favor of bone over uterus. - ACTIVITY - Gynecological; uropathic; antiulcer; hemostatic; osteopathic; cardiant; antiarteriosclerotic; nootropic; neuroprotective; antiinflammatory; antiinfertility; immunomodulatory. - MECHANISM OF ACTION - Estrogen receptor ligand. - The relative binding affinity (estradiol = 100) of (Ia) for rat prostate and uterus estrogen receptors was 50 and 9 respectively, and the ratio of its relative binding affinities for human estrogen receptors alpha and beta was 6 (estradiol = 1).
WO2012125787A1 METHODS FOR TREATING LEUKEMIA AND DISORDERS MEDIATED BY CBFβ AND RUNX1 PROTEINS A method for treating core binding factor (CBF) leukemia in a subject, comprising administering to a subject having CBF leukemia a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt or ester thereof, that inhibits CBFβ and RUNX1 binding in the subject, thereby treating the CBF leukemia.
US20120195987 Substances for reducing occurrence of major cardiac events comprising epa or derivatives thereof, optionally, dha or derivatives thereof and monacolin k Medicaments and therapeutic compositions comprise a composition (1) comprising (A) EPA, pharmaceutically acceptable derivatives of EPA or mixtures thereof, and, optionally, (B) DHA, pharmaceutically acceptable derivatives of DHA or mixtures thereof, wherein the weight ratio of A:B is about 7.5:1 or more, and a composition (2) comprising monacolin K, a source of monacolin K or mixtures thereof. One source of component (1) is fish oil. One source of monacolin K is Red Yeast Rice extract. The compositions are useful for lowering cholesterol and/or triglyceride levels in a subject.
EP2416656A1 Methods for preventing and/or treating lysosomal storage disorders The present invention provides methods for preventing and/or treating lysosomal storage disorders using 5-(fluoromethyl)piperidine-3,4-diol, 5-(chloromethyl)piperidine-3,4-diol, or a pharmaceutically acceptable salt, solvate, or prodrug thereof, or any combination of two or more thereof. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.
US20080268034 High surface area of colloidal silicon dioxide neutralizes the surface charges from the particles which then de-segregate into individual particles, with colloidal silicon dioxide acting as a drug carrier; easily processed into a desired dosage form The present invention relates to solid oral dosage forms of ziprasidone and salts thereof and processes for their preparation, containing colloidal silicon dioxide.
US20080206263 Methods and Compositions for Prognosing, Detecting, and Treating Age-Related Macular Degeneration The invention provides methods and compositions for determining whether a subject is at risk of developing age-related macular degeneration, for example, the wet or neovascular form of age-related macular degeneration. The method involves determining whether the subject has a protective variant and/or a risk variant at a polymorphic site in the HTRA1 gene. In addition, the invention provides a method of treating or slowing the progression of age-related macular degeneration by reducing the expression of the HTRA1 gene, or reducing the biological activity of the HTRA1 gene product.
CN102961388A Medicine capable of promoting secretion of glp-1 and restraining secretion of gip The invention provides an incretin-associated medicine capable of restraining secretion of GIP completely and promoting secretion of GLP-1 and highly safe. The medicine capable of promoting the secretion of GLP-1 (glucagon-like peptide-1) and restraining the secretion of the GIP (glucose-dependent insulinotropic peptide) comprises non-antagonistic inhibitor of clastic enzyme of cane sugar, such as L-gum sugar, D-wood sugar and D-tagatose, as an active ingredient.
EP1986619A2 Use of phosphatases to treat tumors overexpressing n-cor This invention provides a method of treating a patient suffering from a tumor overexpressing N-CoR comprising administering to the patient a phosphatase ligand, alone or in combination with 'a retinoid receptor ligand, a histone deacetylase ligand, or both, in amounts effective to treat the patient. This invention also provides a method of inhibiting tumor growth in a patient suffering from a tumor overexpressing N-CoR. This invention further provides a method of identifying a compound or a mixture of compounds capable of inducing differentiation of cells of a tumor overexpressing N- CoR. This invention still further provides a method of determining the likelihood of successfully treating a subject suffering from a tumor overexpressing N-CoR. This invention also provides a method of assessing the- likelihood that a patient is suffering from a tumor overexpressing N-CoR. This invention yet also provides a method of assessing the likelihood that a patient previously suffering from and treated for a tumor overexpressing N-CoR has suffered a recurrence of a tumor overexpressing N-CoR. Finally, this invention provides analogous methods for use on glioblastoma multiforme.
DE102006050510A1 New substituted dihydropyrazolthione compounds are hypoxia-inducible transcription factor-prolyl-4-hydroxylase inhibitors useful to treat or prevent e.g. heart insufficiency, anemia, chronic kidney diseases and renal failure Substituted dihydropyrazolthione compounds (I) and their salts, solvates and solvate of the salts, are new, where (I) excludes 3-methyl-4-(3-methyl-1,2,4-oxadiazol-5-yl)-1-pyridin-2-yl-1H-pyrazol- 5-thiol. Substituted dihydropyrazolthione compounds of formula (I) and their salts, solvates and solvate of the salts, are new, where (I) excludes 3-methyl-4-(3-methyl-1,2,4-oxadiazol-5-yl)-1-pyridin-2-yl-1H-pyrazol- 5-thiol. R1>, R2>nitrogen containing heteroaryl groups; and R3>H, 1-6C alkyl or 3-7C cycloalkyl. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) preparation of (I); and (2) a medicament comprising (I) in combination with an inert, non-toxic, pharmaceutical auxiliary material. [Image] - ACTIVITY : Cardiovascular-Gen; Cardiant; Antianemic; Antidiabetic; Vasotropic; Nephrotropic; Neuroprotective; Endocrine-Gen; Anabolic; Ophthalmological; Antiparkinsonian; Nootropic; Analgesic; Vulnerary; Cytostatic; Antianginal; Cerebroprotective; Antiarteriosclerotic; Hypotensive; Antiinflammatory; Antimicrobial; Gastrointestinal-Gen.; Antiarthritic; Antirheumatic. - MECHANISM OF ACTION : Hypoxia-inducible transcription factor-prolyl-4-hydroxylase inhibitor. Tests details are described but no results given.
CN102068434A Application of 4-(cyclohexyl)-aminoquinazoline compounds The invention relates to the field of medical immunology, and discloses application of a compound shown as a formula (I) in preparing a medicament used for inducing T cells to be differentiated into FoxP3+CD4+ regulatory T cells and inhibiting the T cells from proliferating, wherein the compound shown as the formula (I) belongs to 4-(cyclohexyl)-aminoquinazoline compounds. The compound shown as the formula (I) plays a remarkable role in inhibiting the T cells from proliferating and inducing the T cells to be differentiated into the FoxP3+CD4+ regulatory T cells, and the medicament which is prepared by the compound and is used for inducing the T cells to be differentiated into the FoxP3+CD4+ regulatory T cells and inhibiting the T cells from proliferating can be used for autoimmune diseases and transplantation rejection.
US20110105575 Method of treatment of hereditary hemochromatosis The present invention relates to the use of Compound I of the following formula in the treatment of iron overload resulting from hereditary hemochromatosis in patient in need of such a treatment and to a commercial package comprising Compound I together with instructions for the treatment of iron overload in hereditary hemochromatosis patients.
WO2014028803A1 Substituted pyrazoles as n-type calcium channel blockers The present invention relates to compounds of Formula (I), wherein X1, X2, X3, X4, R1, R2, R3, and Q are as defined herein, useful as N-type calcium channel blockers.
WO2012113894A1 Pharmaceutical combination of betahistine and trimetazidine This invention is related to pharmaceutical combination of betahistine or pharmaceutically acceptable salts thereof and trimetazidine or pharmaceutically acceptable salts thereof.
CN1857473A Gynostemma pentaphylla saponin composition preparation and its preparing process The present invention relates to compound preparation with gynostemma pentaphylla saponin composition as main component for treating cardiac and cerebral vascular diseases. The gynostemma pentaphylla saponin composition contains gynostemma pentaphylla saponin in 1-99 wt% and ligustrazine, shortscape fleabane herb flavonid, total haw stem and leaf phenolic acid, gingko leaf flavonid, sowthistle-leaf ixeris flavonid, safflower flavonid, pueraria flavonid, total astragalus flavonid and saponin, salvianolic acid, total paeoniflorin or seabuckthorn flavonid in 1-99 wt%, and is compounded with pharmaceutically acceptable supplementary material to prepare pharmaceutically acceptable preparations. The medicine of the present invention is used in preventing and treating cardiac and cerebral vascular diseases, senile dementia, and other diseases.
EP1212295B1 Substituted alpha-hydroxy acid caspase inhibitors and the use thereof The present invention is directed to novel substituted α-hydroxy acid thereof, represented by general Formula (I), where R1-R5, X and Z are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
WO2007031845A2 Polymorphic forms of (s)-omeprazole magnesium salts and processes for their preparation Novel polymorphs of a magnesium salt of (S)-omeprazole trihydrate and processes for their preparation are disclosed. Also disclosed is a process for the preparation of an amorphous form of a magnesium salt of (S)-omeprazole. Pharmaceutical compositions containing the magnesium salts are also disclosed.
EP1737412A2 Use of sulfated hyaluronic acid Disclosed is the use of sulfated hyaluronic acid for inhibiting or treating inflammatory states of the eye, especially blepharitis and conjunctivitis, among other things.
CA2266409C Mouthwash comprising calcium and phosphate ions in supersaturated solution Aqueous solutions are disclosed which are supersaturated with respect to calcium phosphate(s) and which further comprise a stabilising agent in an amount sufficient to enable the calcium ions and phosphate ions to remain in supersaturated solution so that it may be used as a dental rinse or mouthwash. Such solutions are suitable for treating patients having dental caries or other conditions of the oral cavity.
CN102697866A Ultrasonic extraction process for particles for removing urinary calculus The invention relates to the field of natural medicines, in particular to an ultrasonic extraction process for particles for removing urinary calculus. By the process, an ultrasonic extraction technology is applied, the extraction efficiency is improved, and temperature is low; and the ultrasonic extraction process is short in time, low in cost and obvious in economic benefit.
CN101596180A Plant amino acid type chelated calcium, iron and zinc composition and preparation method thereof The invention relates to a plant amino acid type chelated calcium, iron and zinc composition and a preparation method thereof. The plant amino acid type chelated calcium, iron and zinc composition comprises the following substances: plant amino acid, calcium carbonate, ferrous sulfate, zinc sulfate, honey, plant spice and a stabilizing agent. The plant amino acid and a chelate complex series product thereof can deracinate and remove the mutual cross infection of human and livestock together-disease factors caused by using animal amino acid and a chelate complex thereof, and can fundamentally eliminate the efficient path of the mutual cross infection and propagation of human and livestock pathogenic factors and diseases caused by using the animal amino acid and the chelate complex thereof. The invention utilizes plant complex amino acid (produced by using the 200810140536.8 patent technique of the inventer of the invention) to carry out a chelated reaction with calcium carbonate(lactate), ferrous sulfate(lactate) and zinc sulfate(lactate) to produce plant complex amino acid type chelated calcium, chelated iron, chelated zinc or chelated complex products.
CN1879673A An externally applied medicine for treating hicismus by realgar Disclosed is an externally-used medicament for treating body odor which is prepared from the following raw materials (by weight ratio): purslane, red lead, white alum, orpiment, boneol, perfume compound and ethanol.
CN101780174A Internal medicine combined with Chinese and western medicine for curing allergic rhinitis and preparation method thereof The invention relates to an internal medicine combined with Chinese and western medicine for curing allergic rhinitis and a preparation method thereof; 6 to 15 parts of inverted grass, 9 to 15 parts of dandelion, 6 to 12 parts of angelica, 6 to 9 parts of rhizoma ligustici wallichii, 6 to 9 parts of radix sophorae falvescentis, 3 to 6 parts of mint, 9 to 12 parts of fructus xanthil, 6 to 12 parts of burdock-seed, 1 to 9 parts of licorice roots northwest origin, 0.3 to 0.6 part of paracetamol, 0.004 to 0.012 part of chlorpheniramine, 0.3 to 0.6 part of calcium lactate, and 0.3 to 0.9 part of caffeinum natrio benzoicum are prepared in parts by weight for standby use; and the medicine materials are respectively decocted, concentrated, air-dried, crushed, mixed with western medicine to be screened and processed, and tablets or capsules are prepared. The medicine can treat seasonal allergic rhinitis, can remove symptoms and recover the health after being taken for 1 to 2 days, and can cure the diseases after being continuously taken for 6 to 12 days; and can treat patients with seasonal allergy rhinitis, can fully remove the symptoms after being taken for 6 to 12 days, and cure the diseases after the health state is kept for 4 to 8 weeks. The finished medicine can be produced industrially, the dose for a patient is 3 times per day, and 1 to 2g per time. The preparation combined with Chinese and western medicine of the invention not only can diminish inflammation, dissipate blood stasis, invigorate blood circulation, eliminate swelling and enlighten, but also has the effect of desensitization and better clinical effect, and has won the trust of the majority of patients.
WO2009074519A1 Combinations of pyrazolyl or isoxazolyl p2x7 modulators with further therapeutic agents The present invention relates to combination comprising a compound of formula (I) or (IA) or a pharmaceutically acceptable salt thereof: together with a further therapeutic agent or agents. The pyrazolyl (I) and isoxazolyl (IA) compounds of formula (I) and (IA) are thought to be P2X7 receptor antagonists, i.e. to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The further therapeutic agent can e.g. be methotrexate, an NSAID, a TNFα inhibitor, sulfasalazine, a statin, or an anti-CD20 monoclonal antibody, e.g. for the treatment of rheumatoid arthritis; or can be e.g. paracetamol, an opioid, pregabalin, gabapentin, gabapentin enacarbil, or carbamazepine, e.g. for inflammatory or neuropathic pain.
WO2014155103A1 Taurine compositions suitable for inhalation The invention discloses spray-dried compositions for inhalation and methods for preparing such powder compositions. The compositions of the invention are produced by spray-drying taurine under conditions that (i) retain the physical and chemical stability of the composition during spray drying and upon storage, (ii) protect the powder composition from aggregation and (iii) provide particles suitable for aerosolisation.
US7358245 Administering a therapeutically effective amount of a compound which is a cannabinoid receptor agonist, a pharmaceutically acceptable salt of the compound, an isomer of the compound, or a pharmaceutically acceptable salt of the isomer The administration of cannabinoid receptor agonists for inhibition of transient lower esophageal sphincter relaxations, gastroesophageal reflux disease and regurgitation is disclosed.
US20090209571 Phenanthrene derivatives as MPGES-1 inhibitors The invention encompasses novel compounds of Formula or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.
US8304416 Chromenone derivatives Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of tumors, for neuroprotection and for protection of the stress proteins of the skin.
CN102675300A Lipoic acid-aporphine conjugated compound, medicine composite and usage thereof The invention relates to a lipoic acid-aporphine conjugated compound, a medicine composite and the usage thereof, in particular to the lipoic acid-aporphine conjugated compound expressed in the formula I, a stereoisomer of the conjugated compound, salt acceptable to the pharmacy or solvates acceptable to the pharmacy, a medicine composite of the conjugated compound and the usage of the conjugated compound in preparation of medicines for treating central nervous system diseases, wherein the central nervous system diseases include Parkinson's disease, schizophrenosis, depression and drug addiction. The formula I is as follows.
US8664224 External preparation for athlete's foot treatment External preparations for athlete's foot treatment capable of enhancing patient's compliance and capable of reducing the symptom of rubefaction, comprising an anti-trichophyton drug mixed with at least one compound selected from among 1-menthol, menthol analogue compounds and bactericidal compounds.
WO2014086865A1 1-phenyl-2-pyridinyl alkyl alcohol derivatives as phosphodiesterase inhibitors The present invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to 1-phenyl-2-pyridinyl alkyl alcohol derivatives, to processes for the preparation thereof, compositions comprising them, combinations and therapeutic uses thereof.
US20110151014 Microcrystalline cellulose and calcium carbonate compositions useful as recompactible pharmaceutical excipients Coprocessed compositions containing microcrystalline cellulose and calcium carbonate, wherein the weight ratio of microcrystalline cellulose to calcium carbonate is relatively high, are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. Such compositions may be obtained, for example, by preparing aqueous slurries or wet masses of microcrystalline cellulose and calcium carbonate and drying such slurries or wet masses to produce particulate products. The coprocessed products exhibit improved recompactibility, as compared to coprocessed products having lower microcrystalline cellulose:calcium carbonate weight ratios or as compared to physical dry blends of the two excipients.
WO2010137335A1 TURN-OVER-ACCELERATING COMPOSITION CONTAINING α-LIPOIC ACID NANOPARTICLES Disclosed is a composition for accelerating the turn-over of the skin. Specifically disclosed is a composition for accelerating the turn-over of the skin, which contains α-lipoic acid nanoparticles, wherein each of the α-lipoic acid nanoparticles comprises α-lipoic acid, a nonionic surfactant, a bivalent metal ion, and a carbonate ion or a phosphate ion. A specific preferred embodiment of the composition is a composition for excreting melanin from the skin, healing wounds, or accelerating the regeneration of the skin.
US20080045511 3-chloro-5-[6-chloro-2-fluoro-3-(1H-pyrazolo[3,4-c]pyridazin-3-ylmethyl)-phenoxy]-benzonitrile; inhibit HIV reverse transcriptase and are useful for treating Human Immunodeficiency Virus (HIV) mediated diseases The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
CN101879185A Liquid medicament for preventing and treating underarm odor The invention relates to a medicament for removing underarm odor, in particular to a liquid medicament for preventing and curing the underarm odor. The liquid medicament is prepared from the following raw materials in part by weight: 10 to 30 parts of solution of aluminium chloride, 2.5 to 5 parts of potassium iodide, 50 to 75 parts of alcohol, 5 to 20 parts of borneol, 0.3 to 1.2 parts of polyvinyl pyrrolidone, 15 to 30 parts of talcpowder, 1 to 5 parts of menthol and 1 to 3 parts of essence. In the invention, the solution for removing the underarm odor has the effects of cleaning, drying, astriction, sterilization, bacteriostasis, sweat astriction and suppression and syndrome prevention, promotes apocrine glands to normally secrete and thoroughly eliminates internal damp heat. The liquid medicament has the advantages of fast effect, evident and long effect, no toxic or side effect, little skin allergy, safe and convenient use and capacity of eliminating the internal condition for generating the underarm odor. Moreover, medicament ingredients can kill bacteria on underarm skins, inhibit the generation of skin bacteria, eliminate the external environment of the underarm odor and avoid the reoccurring of the underarm odor.
CN202568893U System for preparing multi-vitamin The utility model discloses a system for preparing multi-vitamin. The system comprises a grinder, a three-dimensional motion mixer, a high-efficiency wet type granulator, a high-efficiency boiling drier and a tablet press, wherein the grinder is used for grinding raw materials; the three-dimensional motion mixer is connected with the grinder and can uniformly mix the ground raw materials; the high-efficiency wet type granulator comprises a stirring chamber, a stirring paddle, a chopping cutter, a discharge piston and a 16-mesh nylon net rocking granulator for forming wet granules; the stirring paddle and the chopping cutter are arranged in the stirring chamber, and the stirring chamber is provided with a discharge port; the discharge piston is matched with the discharge port, and the 16-mesh nylon net rocking granulator is connected with the discharge port; the high-efficiency boiling drier is connected with the 16-mesh nylon net rocking granulator and can dry the wet granules; and the tablet press is connected with the high-efficiency boiling drier. The system for preparing multi-vitamin uses the high-efficiency boiling drier to dry the wet granules prepared by the high-efficiency wet type granulator. Compared with the traditional drying by using a baking oven, the wet granules can be uniformly dried.
US6864094 Method of preserving oxygen infusions The present invention provides a method for preserving an oxygen infusion containing an aqueous suspension of molecular assemblies which contain hemoglobin or a heme compound, by: a) modifying the molecular assemblies with polyoxyethylene; and b) converting the hemoglobin or the heme compound into a deoxy-form by removing oxygen from the suspension.
CN102357221A Chinese patent drug lotion for treating fungal infection of hands The invention relates to Chinese patent drug lotion for treating fungal infection of hands, which is composed of garden balsam stem, pepper, radix sophorae flavescentis, cortex dictamni, fructus kochiae, golden cypress, fructus cnidii, radix stemonae, sulpher, safflower carthamus and angelica sinensis. The Chinese patent drug lotion has the effect of being heat-clearing and damp-drying, relieving rheumatic pains and cold, relieving etching, purging intense heat, invigorating the spleen and circulation of blood and the like, is used for treating both the symptoms and the root causes of the fungal infection of hands caused by various reasons and can achieve the aim of enabling the fungal infection of hands not to be prone to reappear.
EP1220689B1 Medicament for the treatment of chronic fatigue syndrome associated with fibromyalgia and irritable bowel syndrome. A method of treatment of disorders of neurological origin and drug formulations for use in the method are disclosed. These conditions comprise fatigue and associated syndromes of pain, weakness and depressed mood which are associated with chronic fatigue syndrome, brain injury and stroke, stress, fibromyalgia, and irritable bowel syndrome. The treatment comprises administering to a patient in need thereof a selective inhibitor of noradrenaline reuptake combined with either phenylalanine or tyrosine in the same dosage form or the same pack. The noradrenergic drug may be selected from lofepramine, desipramine or reboxetine. The selective inhibitor may be a combined inhibitor of both noradrenaline and serotonin reuptake such as venlafaxine, duloxetine or milnacipran, or an inhibitor of both noradrenaline and dopamine reuptake such as bupropion.
CN102631319A Phellinus linteus polysaccharide oral liposome medicine and preparation technology thereof The present invention relates to a Phellinus linteus polysaccharide oral liposome medicine and a preparation technology thereof. By encapsulating the Phellinus linteus polysaccharide by a liposome, after the Phellinus linteus polysaccharide is orally taken and enters the digestive system, the encapsulated Phellinus linteus polysaccharide is prevented from being destroyed by gastric juice, bile and the like, and effectively delivered to the absorption site, therefore, the blood drug level of the Phellinus linteus polysaccharide is increased, and the half-life period of the Phellinus linteus polysaccharide is prolonged. Compared with the Phellinus linteus polysaccharide which is not encapsulated by the liposome, the Phellinus linteus polysaccharide encapsulated by the liposome has the advantages that the blood drug level is increased and the half-life period is obviously prolonged.
US20090111777 Jelly Composition It is intended to provide a composition having at least one effect among the following effects; a plurality of medicinal ingredients can be taken as one preparation and the convenience for patients is excellent; the drug compliance is excellent; the amount of jelly composition to be taken at a time is small; the release of an active ingredient in the digestive tract is excellent; the absorption of an active ingredient to the body is excellent; the storage stability of an active ingredient is excellent; the dispersibility of an active ingredient in the composition is excellent; the storage stability of the composition is excellent; the syneresis of the composition is less, it has an appropriate jelly strength to a degree that does not disintegrate during carrying and before taking and easily disintegrates after taking; the handleability during preparation of the composition is excellent; the portability of the composition is excellent; the feeling of taking the composition is excellent; it has an effect on reducing side effects; and the like. The jelly composition contains a polyvalent unsaturated fatty acid, a second medicinal ingredient, an emulsifying agent and a gelling agent.
EP1568708A2 Methods and medical uses of nucleic acids encoding a TRAF inhibitor The invention concerns novel inhibitors of tumor necrosis factor receptor associated factor-(TRAF) mediated signal transduction. The invention encompasses the novel inhibitor proteins (I-TRAFs), nucleic acid encoding them, medical uses thereof, methods for their recombinant production, and their use in screening assays and as pharmaceuticals.
WO2014002042A1 Injectable supersaturated acetaminophen solution for spinal administration The present invention relates to an acetaminophen injectable aqueous solution for use in the treatment or in the prevention of pain by spinal administration, wherein said acetaminophen injectable solution is supersaturated. In certain embodiments, the acetaminophen injectable aqueous solution is administered simultaneously, separately or sequentially with a local anaesthetic by spinal administration.
CN101691388A Method for preparing anthracycline cytotoxin compound pharmaceutically acceptable salt and application thereof The invention discloses a method for preparing anthracycline cytotoxin compound pharmaceutically acceptable salt and application thereof, and the compound is the compound as shown in general formula (I) or (II). The compound synthesized by anthracycline cytotoxin drugs and organic acid or salt thereof is characterized in that organic acids in the method are selected from organic acids such as formic acid, acetic acid, propionic acid, oxalic acid, butyric acid, malonic acid, succinic acid, fumaric acid, maleic acid, malic acid, tartacit acid, citric acid, picric acid, methylsulfonic acid, ethanesulfonic acid and the like and acidic amino acids such as aspartic acid, glutamic acid and the like or derivatives thereof, and the butyric acid or derivatives thereof, citric acid and succinic acid are preferable. Compared with the original anthracycline cytotoxin compound, the compound has stronger effect of inhibiting tumors and obviously lowered adverse effect and improved safety, and can be used for preparing novel anti-tumor drugs. The preparation method of the compound is simple and is suitable for industrialized production and implementation. In the general formula (I), R1=OCH3 or H, R2=CH2OH or CH3; and in the general formula (II), R1=OCH3 or H, R2=CH2OH or CH3.
US20070155724 Methods of Treating Cytokine Mediated Diseases Disclosed are methods of treating acute and chronic inflammation in the lung caused by inhalation of smoke, endometriosis, Behcet's disease, uveitis, ankylosing spondylitis, pancreatitis, cancer, Lyme disease, sepsis, chronic obstructive pulmonary disease, traumatic arthritis, congestive heart failure and restenosis following percutaneous transluminal coronary angioplasty, known to be cytokine mediated, using aromatic heterocyclic compounds described in WO 00/55139.
US20120122849 Pkm2 modulators for use in the treatment of cancer Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.
CN1823843A Child ammonia phenol alkyl amine affervescent tablet and its preparation method An infantile effervescent tablet of aminophenol alkylamine is prepared proportionally from p-acetylaminopenol, adamantanamine hydrochloride, coffin, artificial bezoar, chlorpheniramine maleate, effervescent agent, filler, flavouring and lubricant.
US20100056444 Treatment of Alzheimer's Disease Using Compounds that Reduce the Activity of Non Selective Ca Activated ATP- Sensitive Cation Channels Regulated by SUR1 Receptors NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time. Exemplary pharmaceutical compositions include compositions including glibenclamide and memantine; glibenclamide and donepezil; tolbutamide and memantine; tolbutamide and donepezil; and these compositions further including glucagon and/or glucose.
EP1684757A1 Substituted piperidines for the treatment of metabolic syndrome The use of compounds of formula (I) wherein variable groups are defined within; in the manufacture of medicaments for use in the inhibition of 11βHSD1, process for making them, certain compounds within the definition of the formula (I) and pharmaceutical compositions comprising them are described. The compounds are useful in the treatment of metabolic syndrome, diabetes and obesity.
US20080260790 Increase acoustic deposits at target using plasmid; nanostructure biocompatible solid; plasmid intensifier comprises a core material encapsulated by membrane in aqueous solution The present invention discloses a plasmid enhancement agent for high intensity focused ultrasound (HIFU) treatment, which can increase acoustic energy deposition at the target location during HIFU treatment. The enhancement agent comprises a nanometer-sized biocompatible solid. The present invention also discloses another plasmid enhancement agent for HIFU treatment, wherein, the enhancement agent comprises a discontinuous phase is comprised of a core material encapsulated by a membrane-forming material, and a continuous phase comprised of aqueous medium; the discontinuous phase is uniformly dispersed in the continuous phase and has a particle size ranging from 10-1000 nm; the amount of the membrane-forming material in the enhancement agent is 0.1-100g/L; and the core material comprises nanometer-sized biocompatible solid selected from the group consisting of magnetic biomaterials, hydroxylapatite, and calcium carbonate, and the amount of the core material in the enhancement agent is 0.1-150 g/L.
US20060128003 Therapeutic agents for low HDL-cholesterolemia The present invention is to provide an agent for low HDL-cholesterolemia, a prophylactic and/or therapeutic antiarteriosclerosis agent as well as a method for preventing and treating low HDL-cholesterolemia, arteriosclerosis and their related diseases or disorders, with emphasis given to improvement in HDL, without resorting to genetic engineering technology. Further, the present invention is to provide a clinically effective agent for low HDL-cholesterolemia and a prophylactic and/or therapeutic antiarteriosclerosis agent, comprising at least one cysteine protease inhibitor as an active ingredient, thereby increasing a quantity of expressed ABCA1 and elevating blood HDL levels, without using the genetic engineering technology.
WO2014037750A1 Inhibitor compounds The present invention relates to compounds of formula (I), wherein R, R, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1 – also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
WO2014104583A1 Process for preparing meropenem trihydrate The present invention provides a process for the preparation of meropenem trihydrate in high purity and high yield, through using a dry methanol solvate of meropenem. The process of the present invention can remarkably reduce the amount of residual solvents in the resulting product, thereby being able to obtain meropenem trihydrate in high purity.
US20100255097 Polysaccharide derivatives of lipoic acid, and their preparation and use as skin cosmetics and medical devices Disclosed are polysaccharides containing residues of glucosamine or galactosamine in the repetitive unit, characterised by the presence of esters on the hydroxyls or amides on the amine functions, with lipoic acid or with mixtures of lipoic acid and formic acid.
CN101585793A Preparation method of sodium dimercaptopropane sulphonate The present invention relates to a preparation method of sodium dimercaptopropane sulphonate, which resolves the problem of long reaction time, low yield and the like of the sodium dimercaptopropane sulphonate preparation with the prior art. The preparation method mainly comprises: bromination reaction, thiolation reaction, salt forming reaction, metal ions removing reaction, refining process and so on. The yield is obviously enhanced due to optimization of the reaction time and raw material ratio.
US20130157950 Method for treating and/or preventing neurodegenerative disease by adiponectin receptor agonist The present invention was accomplished for the purpose of developing a method for effectively treating and/or preventing synucleinopathies, and is based on a discovery that an adiponectin receptor agonist suppresses α (alpha)-synuclein aggregation, tau phosphorylation and a decrease in proteasomal activity. The method of the present invention for treating and/or preventing neurodegenerative diseases includes a step of administering an effective dose of at least one effective element selected from a group consisting of: adiponectin as an adiponectin receptor agonist; a compound inducing expression of adiponectin; globular adiponectin; and a compound inducing expression of globular adiponectin. The present invention further provides a screening method of the adiponectin receptor agonist for treating and/or preventing neurodegenerative diseases.
US7893204 Attractin/mahogany-like polypeptides The present disclosure provides attractin/mahogany-like polypeptides and fragments thereof, polynucleotides encoding such polypeptides and fragments, processes for production of recombinant forms of such polypeptides, antibodies generated against these polypeptides or fragments, and assays and methods employing these polypeptides, antibodies, and polynucleotides.
US7211594 Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith This invention is generally directed to Indazole Derivatives having the following structure: or pharmaceutically acceptable salt thereof, wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of diseases and disorders that are responsive to JNK inhibition, such as an inflammatory disease or disorder. Thus, methods of treating such diseases and disorders are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
CN103202825A Application of curcumin analogue The invention relates to application of a curcumin analogue, and usage of the curcumin analogue as a medicine for inhibiting activity of human type III 17beta-hydroxysteroid dehydrogenase. When used as a medicine, the compound provided by the invention can be used directly in a bulk form, and can also be used in a form of a pharmaceutical composition. The pharmaceutical composition contains 0.1%-99% of the compound provided by the invention, and the balance of a pharmaceutically acceptable carrier or excipient having no toxicity or inertness to human and animal; and the medicinal carrier or excipient is one or more selected from solid, semi-solid, a liquid diluent, a filler and a pharmaceutical product. The medicine provided by the invention can be applied in form of unit weight service amount by a variety of drug delivery ways, such as oral, sublingual, rectal, vein or transdermal, but preferably oral administration.
WO2007065726A1 11β-BENZALDOXIME DERIVATIVES OF D-HOMOOESTRA-4,9-DIEN-3-ONES The present patent application relates to 11β-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones of Formula (I): wherein R1 is a hydrogen atom or a C1-C6-alkyl, C1-C6-acyl, C1-C4-alkoxycarbonyl, C1-C4-alkylthiocarbonyl, C1-C6-alkylaminocarbonyl or arylaminocarbonyl group; and R2 is a hydrogen atom or a C1-C6-alkyl or C1-C6-acyl group. Compounds of Formula (I) bind more strongly to the glucocorticoid receptor than to the progesterone receptor and are effective antiglucocorticoids. According to the invention, they are suitable for the treatment and/or prevention of symptoms and/or diseases that are attributable to an androgen deficiency induced by glucocorticoids, especially cortisol.
CN102743367A Application of liquidambar formosana hance fruit tannin monomer The invention relates to applications of liquidambar formosana hance fruit tannin monomer. The monomer comprises the components of gallic acid, ethyl gallate, p-digalloyl acid, and ethyl-p-digallate. The invention relates to the application of the monomer in preparing a monoamine oxidase inhibitor. The invention is characterized in that the invention relates to the applications of gallic acid, ethyl gallate, p-digalloyl acid, and ethyl-p-digallate in preparing medicines used for treating depression and Parkinson's disease.
CN102872093A Application of Houttuynoid E in medicine for treating pancreatic cancer The invention discloses application of Houttuynoid E in preparing a medicine for treating pancreatic cancer, belonging to the technical field of new application of a medicine. According to the invention, the in-vitro MTT anti-tumor activity evaluation discovers that the Houttuynoid E also has an obvious effect on suppressing the growth of the human pancreatic cancer cell strains PANC-1 and BXPC-3. Thus, the Houttuynoid E can be used for preparing an anti-pancreatic cancer medicine and has good prospects in development and application. The application of Houttuynoid E in preparing a medicine for treating pancreatic cancer is disclosed for the first time; and the skeleton type is a brand new one, and the activity in suppressing pancreatic cancer cells is unexpectedly strong.
CN103058995A Quinazolinyl piperazine derivative and purpose thereof The invention belongs to the technical field of medicine, and relates to a quinazolinyl piperazine derivative and a purpose thereof. The derivative provided by the invention has a following general formula as shown in the specification, wherein R1 is hydrogen, halogen, (C1-C4) alkoxy and methoxy (C1-C4) alkoxy; R2 is hydrogen, (C1-C4) alkoxy and methoxy (C1-C4) alkoxy; R3 is hydrogen, C5-C10 aryl and (C1-C4) alkyl; R4 is C5-C10 aryl, C5-C10 heteroaryl and C5-C10 heteroaryl (C1-C4) alkyl, wherein the heteroaryl contains 1-3 heteroatoms selected from O, N and S, and R4 is optionally substituted by 1-3 of R5; and R5 is hydrogen, halogen, hydroxyl, trifluoromethyl, trifluoromethoxy, amino, nitro, (C1-C4) alkyl, (C1-C4) alkyl alkenyl, (C1-C4) alkynyl, (C1-C4) alkoxy, hydroxy (C1-C4) alkyl, allyl, (2-methyl) propyl, (C1-C4) alkoxymethyl, aryl (C1-C4) alkyl and aryl (C1-C4) alkoxy. The quinazolinyl piperazine derivative provided by the invention has relatively good antineoplastic activity.
CN103242332A 1-N acyl substituted indolone derivative The invention belongs to the technical field of drug synthesis and relates to a novel 1-N acyl substituted indolone derivative as well as a preparation method and an application thereof. According to the invention, the 1-N acyl substituted indolone derivative with the potential biological activity is obtained for the first time through taking 4-bromaniline as a starting material and being subjected to oxime forming, cyclization, acetal protection and N-alkylation reactions.
US20090155319 Method for producing cosmetic and/or dermatological powder A cosmetic or dermatological powder, which comprises (i) from 61 to 99.99% by weight is relative to the total weight of the powder of at least one starch modified by a combination of esterification and heat-moisture treatment, (ii) from 0.01 to 29.99% by weight is relative to the total weight of the powder, of an oily phase comprising at least one oil.
US20100105692 Dipterinyl Calcium Pentahydrate (DCP) and Therapeutic Methods Based Thereon Provided herein is dipterinyl calcium pentahydrate (DCP) and therapeutic methods based thereon. Also provided herein is the compound dipterinyl calcium pentahydrate (DCP) or an analog or polymorph thereof.
US20120225052 Composition and method for treating tissue defects The present invention provides a composition and method for treating tissue defects. The composition includes thrombin and fibrinogen, or sodium alginate and calcium chloride, and also a surfactant, and non-resorbable polymer microparticles dispersed within the composition.
CN1754879A Imidazole derivative compound, its salts and use thereof The invention provides compounds and their salts having the formula of (I), and the process for preparing these compounds, wherein D, R1, R2, R22, R21 are defined in the description, they have shown evident effects for anti-ulcer and inhibition of viscera acid secretion, lower toxicity, higher acid resistance, and longer acting time.
US6989377 Treating vitamin D responsive diseases The present invention relates to therapeutics for the prevention and treatment of vitamin D responsive diseases in humans, as well as other animals, through the use of biologically active vitamin D compounds in combination with at least one other immunomodulatory compound such as interleukin-10, interleukin-4, or a TNFα inhibitor.
CN102961379A Rifampicin and anethol trithione compound preparation The invention provides a rifampicin anethol trithione compound preparation, and relates to the technical fields of medicine and medicine manufacturing. The compound preparation comprises the following components in percentage by weight: 0.1-99.9 percent of rifampicin and 99.9-0.1 percent of anethol trithione. The rifampicin and the anethol trithione have a good coordination function; and by the anethol trithione, the cell capability is improved, and liver injury caused by the rifampicin can be effectively treated by increasing choleresis. The rifampicin and the anethol trithione are compounded, so that a good treatment effect on tuberculosis patients is achieved, the adverse reaction of the rifampicin also can be reduced, and the liver injury caused by the rifampicin can be reduced.
US20080206170 Creatine compositions for skin treatment The present invention relates to the use of creatine compounds, such as, for example, creatine monohydrate, creatine pyruvate and creatine ascorbate, for the treatment of skin.
US20080146627 Thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives, e.g., butyl 2-(4-[1,1'-biphenyl]-4-yl-1H-imidazol-2-yl)ethylcarbamate inhibit lipidic peroxidation and monoamine oxidase and modulate sodium channels and are used for treating neurodegenerative disorders or pain. The invention relates to thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives of general formula (I) wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is notably selected from various optionally substituted aromatic radicals, B is notably hydrogen, alkyl or phenyl, R1 and R2 are notably independently hydrogen, alkyl or cycloalkyl and Q is —NR46R47 or —OR48, R46 and R47 are notably independently hydrogen, alkyl, cycloalkyl or —(CH2)k—COOR51, R51 is notably alkyl or haloalkyl and R48 is notably hydrogen or alkyl. These compounds have advantageous pharmacological properties which allow their use in therapeutics, notably for treating neurodegenerative disorders or pain.
WO2007071313A2 Combination of anticholinergics, glucocorticoids, beta2-ag0nists, pde4 inhibitor and antileukotriene for the treatment of inflammatory diseases The invention relates to novel combinations based on anticholinergics, β2-adrenoceptor agonists, PDE 4 Inhibitors, glucocorticoids, and leukotriene-receptor antagonists, process for their production and their use for the treatment of inflammatory diseases, preferably respiratory diseases as bronchial asthma and chronic obstructive pulmonary diseases (COPD) or rheumatic or autoimmune diseases.
US7361459 Antiviral inhibition of capsid proteins Methods for evaluating the antiviral activity of test compounds are provided. Further aspects of the methods involve the retroviral capsid protein of HIV-1. In another aspect, methods of reducing mortality associated with AIDS with a compound that binds to the apical cleft near the C-terminal end of the N-terminal domain of the HIV-1 capsid protein are provided. Derivatives of CAP-1, CAP-2, CAP-3, CAP-4, CAP-5, CAP-6 and CAP-7 are described that bind to the apical cleft of the N-terminal domain of the HIV-1 capsid protein and inhibit proper assembly of the core particle.
US20110195927 Compositions Comprising Polymers Having Amino Sugar Units and Methods of Making and Using Same Compositions comprise a polymer having units of an amino sugar, a polyol other than sorbitol, and boric acid, a salt thereof, or a combination thereof. Such compositions remain for an extended period in the eye and can be used for relief, treatment, or control of a condition of dry eye or discomfort resulting therefrom.
US20120309759 Screening Method and Compounds for Modulating Telomerase Activity The present invention embraces methods for identifying compounds that modulate the activity of telomerase. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the TRBD, “thumb,” “finger,” and/or “palm” domain; or FP-pocket, PT-pocket or Th-pocket of telomerase and testing the compound for its ability to modulate the activity of telomerase. Compounds selected for interacting with the T-pocket or Fingers-Palm pocket of telomerase are also provided.
US20090105240 Methods for treating leukemia and myelodysplastic syndrome, and methods for identifying agents for treating same The present disclosure relates to methods for treating leukemia, pre-leukemic conditions, as well as myelodysplastic syndrome and acute myelogenous leukemia. The present disclosure further relates to compounds that can be used for treating leukemia, pre-leukemic conditions, as well as myelodysplastic syndrome and acute myelogenous leukemia. The present disclosure also relates to methods for identifying compounds that can be used for treating leukemia, pre-leukemic conditions, as well as myelodysplastic syndrome.
CN101659676B Sulfo-Adefovir and Tenofovir liver targeting ester prodrug The invention discloses a sulfo-Adefovir and Tenofovir liver targeting ester prodrug represented by the following general formula (I), or medicinal salt, hydrate or solvate thereof, which serves as the effective component of hepatitis B antivirus. The compound of the invention has liver targeting characteristic and better achieves the aim of small dose, high effect and low toxic or side effect.
US20070218056 Methods for identification, diagnosis, and treatment of breast cancer The invention provides methods of identifying premalignant and malignant breast cancer, determining lymph node involvement in patients diagnosed with premalignant and malignant breast cancer growths, and methods of treating premalignant and malignant breast cancer. The diagnostic and methods comprise intraductal administration of a targeting molecule either alone acting as an identifying agent, or coupled to an identifying agent; the therapeutic methods comprise intraductal administration of a targeting molecule coupled to a therapeutic agent or administration of a targeting molecule having therapeutic activity in and of itself.
WO2009111603A2 Deitary supplement for eye health Nutritional supplements for eye health comprising: an anti-oxidant component; an anti-inflammatory component; and an anti-angiogenic component. The supplements inhibit development and progression of a range of retinal diseases and degenerations, particularly AMD and diabetic eye disease, diabetic retinopathy and diabetic macular edema. The supplements include tocotrienol and green tea extract.
CN102872173A Compound acetaminophen orally disintegrating tablet for beasts and birds and preparation method for compound acetaminophen orally disintegrating tablet The invention relates to a compound acetaminophen orally disintegrating tablet for beasts and birds. The compound acetaminophen orally disintegrating tablet for the beasts and birds consists of the following components in parts by weight: 80-100 parts of acetaminophen, 8-12 parts of Bupleurum sinensis extract, 10-40 parts of polyacrylic resin, 20-60 parts of microcrystalline cellulose, 30-60 parts of polyvinylpolypyrrolidone, 10-30 parts of lactose, 40-60 parts of mannitol, 0.5-2.0 parts of acesulfame and 0.5-2.0 parts of magnesium stearate. The acetaminophen and the Bupleurum sinensis extract are scientifically formulated to prepare the orally disintegrating tablet, and the orally disintegrating tablet can be widely used for treating fever, courbature and rheumatism of horses, cattle, sheep and pigs. The acetaminophen with a bitter taste is treated by the polyacrylic resin by adopting the powder coating technique to better achieve the goal of covering the bitter taste. The compound acetaminophen orally disintegrating tablet for the beasts and birds is rapid in absorption, high in bioavailability, simple in production equipment and low in cost, and a new way is opened for domestic veterinary drug markets to treat acute diseases.
CN103006687A Functional preparation for laser postoperative skin regeneration and preparation method The invention provides a functional preparation for laser postoperative skin regeneration. The functional preparation is characterized by comprising the following components by weight as raw materials of: 0.2-1 part of sodium hyaluronate and 99.8-99 parts of de-ionized water. The preparation method comprises the following steps of: adding the de-ionized water in a water pot, heating to a temperature of 75-80 DEG C, carrying out thermal insulation for 30-35 min, and cooling to a temperature of 40-45 DEG C; adding the main material of the sodium hyaluronate into the pot; and discharging after stirring for 20-30 min, standing, filling and packaging. The functional preparation containing the sodium hyaluronate provided by the invention has the functions of supplying cuticle water, recovering a skin barrier function and promoting laser postoperative skin wound regeneration.
US20120093880 Method and kit for topical elimination of psoriatic lesions with a caustic applicator A method and kit for eliminating a psoriatic lesion involves removal of loose psoriatic scales if present, and moistening remaining scales to a depth to or just above epidermal tissue underlying the scales. The hydrated scales are then contacted with a dry composition of from about 50% to about 95% silver nitrate using a specially configured applicator such that a portion of the moisture of the hydrated psoriatic scales will be absorbed into the dry composition so as to dissolve an outer layer of the silver nitrate into a solution. The solution will then be absorbed into the psoriatic scales to the depth of the moistening thereof to chemically cauterize the moistened scales. The method can be repeated until elimination is achieved. Cauterization of surrounding and underlying tissue is undesirable, and if contacted by moisture, dehydration can be allowed, and the lesion rehydrated as necessary.
WO2008063548A3 5, 6, or 7-substituted-s- (hetero)arylisoquinolinamine derivatives as antitumor agents The present invention relates to 5, 6, or 7-substituted-3-(hetero)arylisoquinolinamine derivatives represented by general formula D, their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included. Formula (I).
WO2013014654A4 Formulas comprising highly soluble elements and vitamin for the prevention and amelioration of osteoporosis The present invention provides methods of producing dosage forms for formulas of elemental compositions encompassing acetate salts of calcium, magnesium and zinc along with vitamin D 3. The acetate salts could be extracted from natural sources such as pearls, coral, and oyster or compounded using synthetic materials. The dosage and ratio of calcium to magnesium was estimated using in vitro and in vivo estimations. The dosage for promoting bone health and alleviation of osteoporosis is about a quarter to a third of the conventional dose.
CN103159826A Lys and Lys (Pro-Ala-Lys)-modified curcumin derivatives, and synthesis and medical application thereof The present invention discloses four pseudo peptides of a formula I, wherein R1 is H or CH3, and R2 is Lys or Lys (Pro-Ala-Lys). The present invention further discloses a preparation method and use thereof. The pseudo peptides of the present invention have excellent thrombolytic activity, antithrombotic activity, anti-inflammatory activity, and OH radical scavenging activity, and a nanostructure.
WO2008127585A1 Substituted furo[2,3-b]pyridine derivatives as cannabinoid-1 receptor modulators Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.
CN101049319A Composition for improving remembrance A composition for improving memory, decreasing blood fat, and preventing and treating cardiovascular and cerebrovascular diseases contains lecithin and fish oil.
US20110104274 Novel composition and uses thereof, in particular cosmetic uses, for treating skin dehydration The present invention relates to the use of a combination comprising gamma-linolenic acid and at least one green tea polyphenol, in which the ratio of the gamma-linolenic acid to the green tea polyphenol ranges from approximately 1 to approximately 10, for increasing the in vitro and ex vivo differentiation of keratinocytes.
CN102120737A Baicalein derivatives and preparation method and application thereof The invention discloses a kind of baicalein derivatives and a preparation method and application thereof. Pharmacological tests prove that the compounds have the obvious function of dilating bronchi and can be used to prepare the medicines used for preventing or curing chronic obstructive emphysema caused by bronchial constriction.
WO2008092352A1 Antitumor compounds and their preparation method The invention provides new antitumor compounds, which are heterocyclic ketone (alcohol) or their derivatives having the structure of formula I. The compounds provided in the present invention can be used for preparing microtubulin protein inhibitors and have antitumor effect, and the invention also provides antitumor pharmaceutical compositions containing the said new compounds as active ingredient. The invention also provides the preparation method for the said compounds. The said compounds of formula I show the advantages of having a small molecular weight, being easy to synthesis and having less poison side effect.
US20130018009 Anti-obesity product and its method of preparation The present invention relates to compositions comprising one or more anthraquinones for use in the treatment of obesity and related metabolic and liver disease. More particularly it relates to a plant extract fraction rich in anthraquinones including both anthraquinone glycosides and anthraquinone aglycones obtainable from a member of the Leguminosae family, more particularly Cassia seeds. It also relates to a method of obtaining a plant extract fraction rich in anthraquinones.
US20050164980 Endcapped block polymers including ethylene oxide-propylene oxide, glycolic acid-lactic acid, or ethylene oxide-lactic or glycolic acid; low viscosity allows easy injection; capable of room temperature distribution; extended analgesic effectiveness; nontoxic antiarthritic agents; tissue repair The present invention provides a safe hyaluronic acid base material that is suitable for use in practical hyaluronic acid pharmaceutical preparations capable of distribution at room temperature and having such a low viscosity that injection is easy. The hyaluronic acid pharmaceutical preparations can reside in a joint cavity for a prolonged period of time while exhibiting analgesic effects. More specfically, there is provide a hyaluronic acid modification product in which hyaluronic acid and/or a pharmaceutically acceptable salt thereof is bounded to a block polymer selected from PEO-PPO-PEO, PPO-PEO-PPO, PEO-PLGA-PEO, PLGA-PEO-PLGA, PEO-PLA-PEO and PLA-PEO-PLA. The hyaluronic acid modification product, despite capability of distribution at room temperature and ease in handling because of the low viscosity, can have its viscoelasticity rapidly increased after injection into a living body, so that it is highly useful in treatment of joint diseases, aid in surgical operation, repair of tissue, etc. as a main ingredient of novel and practical hyaluronic acid pharmaceutical preparations.
US20070173461 Glycoside prodrug of 5- aminosalicylic acid An object of the present invention is to provide a therapeutic agent for ulcerative colitis which allows 5-aminosalicylic acid (5-ASA) useful as a therapeutic agent for ulcerative colitis to be efficiently delivered to the large intestine of the affected site almost without being absorbed or metabolized in the stomach or the upper part of the small intestine and is safe and can be administered over a long term. The present invention relates to 5-ASA into which D-galactose represented by the following general formula [1] has been introduced. The compound of the present invention can be efficiently delivered to the large intestine of the site of action, and is degraded by the intestinal bacterial flora, whereby 5-ASA as the active ingredient can be produced in the large intestine.
CN101317910A Medicament for treatment of stomach disease and preparation method thereof The present invention discloses a medicine for treating stomach diseases, in particular to the medicine and a preparation method thereof for treating stomach diseases such as gastric ulcer, duodenal ulcer and chronic gastritis. The present invention takes celandine, corktree bark, cuttlebone, white alum and menthol as the raw materials, and the medicine is prepared according to proportions. Different herbs are smashed, decocted, filtered, concentrated and dried; then dextrin is added; the menthol is added with a few amount of ethanol and then sprayed into granules for evenly mixing; magnesium stearate is added for evenly mixing, pressing and coating. The medicine provided by the present invention directly contacts disease positions and has the advantages of short curing period, taking effect rapidly, high curing effect and no dependence on the medicine.
US20080312268 Substituted tricyclic piperidone compounds Substituted tricyclic piperidone derivatives corresponding to Formula I: a method for producing such compounds; pharmaceutical compositions containing such compounds, and the use of such compounds to treat pain, depression, urinary incontinence, diarrhea, pruritus, alcohol and drug abuse, drug dependency, lethargy and/or anxiety.
CN101928246A N-[(1-aryl-3-substituted phenyl-pyrazol-4-yl) methenyl]-2-hydroxyl benzoyl hydrazine compound or pharmaceutically acceptable salts and preparation method thereof The invention provides an N-[(1-aryl-3-substituted phenyl-pyrazol-4-yl) methenyl]-2-hydroxyl benzoyl hydrazine compound in a formula (IV) or pharmaceutically acceptable salts and a preparation method thereof. The preparation method comprises the following steps of: diazotizing and reducing arylamine as a raw material, condensing with a product obtained from diazotizing and reducing for Vilsmeier-Haak reaction to obtain 1-aryl-3-phenyl-4-formoxyl pyrazol; and then reacting the 1-aryl-3-phenyl-4-formoxyl pyrazol with salicylyl hydrazine to obtain the N-[(1-aryl-3-substituted phenyl-pyrazol-4-yl) methenyl]-2-hydroxyl benzoyl hydrazine compound shown as the following general formula, wherein each substituent in the formula is defined in the specification. The compound has a good application prospect at the aspect of resisting fungi and Gram negative bacteria.
WO2013047958A1 Composition for inhibiting liver function deterioration, containing citrus peel extract or narirutin as active ingredient, and method for extracting narirutin from citrus peel The present invention relates to a pharmaceutical composition for treating liver diseases, containing a narirutin extract of citrus peel extract or narirutin as an active ingredient. The extract or narirutin decreases cholesterol levels and fat levels in liver tissue, and thus can be utilized as a composition or food for preventing and treating liver diseases. In addition, the present invention relates to a method for extracting narirutin from citrus peel, and a method for preparing citrus fermented milk using the same.
CN103230592A Composition of statin medicine and 5-methyltetrahydrofolic acid, and application thereof The invention relates to a medicine composition composed of 0.1-100mg of one of statin lipid regulation medicines, 0.1-5mg of 5-methyltetrahydrofolic acid, and a pharmaceutically acceptable carrier. The invention also provides an application of the medicine composition in preparing medicines used for treating diseases related to hyperlipidemia or dyslipidemia. The composition provided by the invention has the advantages that: with the medicine composition, statin lipid-regulation medicine treatment effect can be improved. The effect is substantially better than other independent-use statin lipid-regulation medicines in the respect of reducing side effects such as transaminase elevation and myopathy caused by long-term and/or large-dose applications of statin medicines, and toxicity is not increased. Also, the composition is more convenient to take. With the composition, medical cost is reduced, and patient compliance is improved.
US20080045499 Preferential Inhibition of Presenilin-1 The invention provides methods for determining whether an agent preferentially inhibits Presenilin-1-comprised γ-secretase relative to Presenilin-2-comprised γ-secretase. The invention also provides agents that preferentially inhibit Presenilin-1-comprised γ-secretase relative to Presenilin-2-comprised γ-secretase, pharmaceutical compositions comprising such compounds, and methods of treating Alzheimer's disease using such compounds. The invention also discloses that the N-terminal domain of presenilin-1 and -2 determines the difference in the production of Aβ by PS1-comprised and PS2-comprised gamma secretases. This finding identified the structural determinant for the observed difference in the production of Aβ by PS1-comprised and PS2-comprised gamma secretases. Such structural determinant was not identified before. This invention also provides a method for determining whether an agent specifically binds the N terminus of PS1. The invention further provides for methods of treatment of Alzheimer's Disease by administration of an effective dose of an agent which specifically binds PS1, thereby inhibiting PS1 activity.
EP1333842B1 Use of cortisol-sequestering agents for the treatment of hypercortisolaemia related disorders The invention relates to the use of cortisol-sequestering agents for the preparation of a medicament for the treatment of hypercortisolaemia related disorders, especially for the treatment of major depression; to pharmaceutical compositions comprising a cortisol-sequestering agent, and to the cortisol-sequestering agent 6-per-deoxy-6-per-(2,3-dihydroxypropylthio)-η-cyclodextrin.
CN101596171B Tamsulosin sustained release tablet and preparation method thereof The invention provides a Tamsulosin tablet, which is prepared by the following steps: taking Tamsulosin, and dissolving in ethanol; adding a part of hydroxypropyl methyl cellulose and other proper excipients, evenly mixing, and pelletizing; and then adding the rest hydroxypropyl methyl cellulose, fully mixing, and pressing into the sustained release tablet. The release of the Tamsulosin tablet intwo hours is effectively controlled within 40 percent, and the sustained release performance of the medicament is greatly improved. The preparation method has simple adopted equipment and concise production process.
US8518694 Nucleic acid vector comprising a promoter and a sequence encoding a polypeptide from the endogenous retrovirus PCAV A nucleic acid vector comprising: (i) a promoter; (ii) a sequence encoding a HML-2 polypeptide operably linked to said promoter; and (iii) a selectable marker. Preferred vectors comprise: (I) a eukaryotic promoter; (ii) a sequence encoding a HML-2 polypeptide downstream of and operably linked to said promoter, (iii) a prokaryotic selectable marker; (iv) a prokaryotic origin of replication; and (v) a eukaryotic transcription terminator downstream of and operably linked to said sequence encoding a HML-2 polypeptide. Vectors of the invention are particularly useful for expression of HML-2 polypeptides either in vitro (e.g. for later purification). Or in vivo (e.g. for nucleic acid immunization). They are well suited to nucleic acid immunization against prostrate tumors. A preferred HML-2 is PCAV, which is located in chromosome 22 at 20.428 megabases (22q11.2).
CN101933912A Preparation technology of tryptanthrin sustained-release capsule and application thereof The invention provides a preparation technology of tryptanthrin sustained-release capsule which treats tumour, such as leukemia and the like, colitis and fungal infection and application thereof, belonging to the fields of pharmaceutical manufacture and clinical application. The invention is characterized in that tryptanthrin has the action on killing and inhibiting tumour cells, animal transplantable tumour, various fungus and bacteria, has the action on inhibiting inflammation, and has pharmacological activity on regulating immunological functions and the like. The tryptanthrin is prepared into the tryptanthrin sustained-release capsule for serving as drug for resisting tumour, such as leukemia and the like and treating diseases, such as colitis, fungal infection and the like. The tryptanthrin sustained-release capsule has stable drug, controllable quality, high bioavailability, small dosage, actual curative effect, low side effect, abundant raw material resource and low production cost.
CN103717609A Tricyclic inhibitors of poly(adp-ribose)polymerase The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-l(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The invention also shows good cellular activity in inhibiting poly(ADP- ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.
CA2117490C Purified vacuolating toxin from helicobacter pylori and methods to use same This invention relates to a purified Helicobacter pylori vacuolating toxin and methods to use this toxin to produce protective antibodies against H. pylori infection. Antiserum to this antigen can be used to detect the toxin. Methods to detect anti-toxin antibodies determine the susceptibility of a patient to develop peptic ulcer disease, gastric carcinoma, or other clinical consequences of H. pylori infection.
US20120156289 Biodegradable Osmotic Pump Implant For Drug Delivery The present disclosure relates to a drug delivery device including a biodegradable housing and a hydrogel within the biodegradable housing. The housing, the hydrogel, or both, may include a bioactive agent. Also disclosed is a method of drug delivery including the steps of forming the biodegradable housing, in embodiments a hydrogel, suspending a bioactive agent in the hydrogel, and introducing a second hydrogel and/or precursors of a second hydrogel into the biodegradable housing.
CN103387277A Acidic electrolyzed water and composition thereof The invention discloses acidic electrolyzed water and a composition containing the acidic electrolyzed water. The weakly acidic electrolyzed water with low conductivity and high oxidation potential has clear antibacterial, anti-inflammatory, anti-oxidation, and wound-healing-promoting effects. The electrolyzed water has no cytotoxicity, and does not cause allergy. It is proofed that the electrolyzed water can inhibit skin melanoma cancer cell proliferation and migration. Therefore, the acidic electrolyzed water and composition thereof can be safely applied in cosmetic compositions, medical compositions, or other compositions used in skin surface disinfection.
WO2014140159A1 Dosage form comprising crizotinib The invention relates to a method of preparing a tablet, preferably a tablet for immediate release and having a high drug load, containing crizotinib in form of the free base and lubricant, both in specific amounts. The invention further relates to a tablet obtainable by said method.
EP0933993B1 Substituted cyclopentane compounds useful as neuraminidase inhibitors Compounds represented by formula (I), and pharmaceutically acceptacle salts thereof; and their method of preparation are provided. Compounds of the above formula are influenza virus neuraminidase inhibitors and can be used in treating patients infected with influenza virus.
CN1759887A Mucous membrane absorption ingestion type medicinal composition for drawing out interferon, and preparation A mucosa absorption type medicinal composition for inducing interferon contains the polymyocell or its derivative and one or more of the pharmacologically acceptable salts and the polycationic compound and one or more of the pharmacologically acceptable salts. Its preparation in the form of solution, aerosol, spray, or powder for inducing the immune system to generate interferon is also disclosed.
CN1566160A Mu Shen polysaccharide and its immunoregulation and anticancer function The invention provides a process for industrially extracting ginseng polysaccharides, wherein the substantial immunoregulation and tumor inhibition of the ginseng polysaccharides has been disclosed in the invention.
WO2006127217A2 Cyclopropanecarboxylate esters of acyclovir The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, methods of using the same, processes for preparing the same, and intermediates thereof.
US20100111898 Conjoint therapy for treating fibrotic diseases The present invention relates to improved methods of treating fibrotic or fibroproliferative disorders. Conjoint therapies are provided comprising the combination of one or more fibrocyte suppressors and one or more profibrotic factor antagonists or anti-fibrotic agents.
CN103254120A Spiro-azasugar quaternary ammonium salt compound, and preparation method and application thereof The invention discloses a spiro-azasugar quaternary ammonium salt compound, and a preparation method and an application thereof. The structure of the spiro-azasugar quaternary ammonium salt compound is shown in a formula I. The preparation method of the spiro-azasugar quaternary ammonium salt compound provided by the invention is simple, the sipro-azasugar quaternary ammonium salt compound can be used as a glycosidase inhibitor, a drug for preventing and/or treating diabetes, a drug for preventing and/or treating Gaucher's disease, a drug for preventing and/or treating tumor and an antiviral drug.
CN101829081A Application of chromane compound HEF-05 in relaxing smooth muscle of blood vessel The invention relates to the technical field of medicament, and mainly relates to application of chromane compound HEF-05 in preparing a vasodilator, a potassium channel opener, a calcium channel blocker and an endothelium relaxing factor releasing agent. In an animal in-vitro experiment, HEF-05 can relax the contraction of the smooth muscle of the blood vessel of rabbits caused by barium chloride, norepinephrine and potassium chloride. In addition, in a pilot study of a relaxing mechanism, the relaxation function of the HEF-05 is inhibited after the smooth muscle of the blood vessel is incubated by the ATP-sensitive potassium channel blocker glibenclamide. After methyleneblue is added to incubate, the relaxation function of the HEF-05 can be enhanced; and after the HEF-05 is added to incubate, the dose-response curve of the calcium chloride is descended. Therefore, the HEF-05 can be used for preparing a preparation for relaxing the smooth muscle of the blood vessel and can be used as the potassium channel opener, the calcium channel blocker and the endothelium relaxing factor releasing agent.
CA2176117C Generation of high titers of recombinant aav vectors AAV vectors may have utility for gene therapy but heretofore a significant obstacle has been the in-ability to generate sufficient quantities of such recom-binant vectors in amounts that would be clinically useful for human gene therapy application. Stable, helper-free AAV packaging cell lines have been elusive, mainly due to the activities of Rep protein, which down-regulates its own expression and reverses cellular immortaliza-tion. This invention provides packaging systems and processes for packaging AAV vectors that effectively circumvent these problems by replacing the AAV p5 promoter with a heterologous promoter (as depicted in the figure) and that allow for substantially increased packaging efficiency.
US7223772 Cyclooxygenase-2 inhibitors (COX-2); 4-[2-(3-fluoro-phenyl)-6-trifluoromethyl-pyrazolo[1,5-a]pyridin-3-yl]benzenesulfonamide for example; fever, pain, inflammation, neurodegenerative disorders, oral diseases, influenza, arthritis, allergies The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from the group consisting of H, halogen, C1-6alkyl, C1-6alkoxy, and C1-6alkoxy substituted by one or more fluorine atoms; R2 is selected from the group consisting of H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, and C1-6alkoxy substituted by one or more fluorine atoms; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
CN1597689A Ledebouriella root glycoside and its preparation and application A solerioside A used to prepare the medicine for preventing and treating the diseases associated with the unbalance of oestrogen or progestogen is prepared from the Guandong ledebouriella root through extracting and separation.
WO2005013954A1 Modified release venlafaxine hydrochloride tablets A modified release tablet of venlafaxine hydrochloride is formed by a core containing a lipophilic matrix and venlafaxine hydroochloride and a water-insoluble, permeable coating thereover.
US7014652 Methods for treating prostatitis Methods, systems, and computer program products for providing thermal therapies or internal thermal massage therapy for treating prostatitis by expanding and contracting a treatment balloon with inflation media and currently applying heat to a portion of the prostatic urethra.
EP2528897A1 Di - substituted pyridine derivatives as anticancers The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].
WO2007082546A1 Use of tofisopam as a pde10a inhibitor The present invention relates to a novel use of Tofisopam for the preparation of a pharmaceutical composition made for treatment of the positivsymptoms and cognitive deficits in schizophrenic patients.
CN103239465A Application of quercetin-3-O-alpha-L-rhamnose-3'-alpha-L-rhamnoside in preparation of medicine for treating cardiovascular and cerebrovascular diseases The invention relates to application of quercetin-3-O-alpha-L-rhamnose-3'-alpha-L-rhamnoside (quercetin3, 3'-di-O-alpha-L-rhamnoside) in the aspect of treating cardiovascular and cerebrovascular diseases.
CN102793660A Etofesalamide ointment and preparation technology thereof The invention relates to an ointment for the treatment of eczema and neurodermatitis, and concretely relates to an etofesalamide ointment. The ointment comprises a therapeutically effective amount of the etofesalamide ointment, and pharmaceutically acceptable excipients; and the ointment further comprises a hydrophilic gel material and a skin penetration enhancer. The hydrophilic gel material is carbomer resin, and the skin penetration enhancer is macrogolglyceride. Compared with the prior art, the technology improves penetration rate of the drug through skin. The ointment prepared by the technology has the characteristics of being not greasy and easy to clean, and does not affect the normal function of the skin, can promote the excretion of eczema secretion, and thereby significantly improves compliance of patients. The technology is simple and feasible, and easy to realize.
CN103371976A Celecoxib-containing solid dispersion and preparation method thereof The invention provides a celecoxib-containing solid dispersion and a preparation method thereof. The celecoxib-containing solid dispersion comprises celecoxib and copovidone. The celecoxib-containing solid dispersion provided by the invention has the advantages of high rigidity, good friability and moderate glass temperature, can be suitable for large-scale industrialized production and overcomes the defects of low glass temperature, soft material, easy melting and bonding, difficulty in crushing and the like of a celecoxib solid dispersion which takes polyethylene glycol as a carrier.
US7745455 Administrating a first cytidine analogue reverse transcriptase inhibitor concurrently with deoxycytidine; increasing the antiretroviral activity of the first analogue; HIV treatment Boosted cytidine analogue reverse transcriptase inhibitor antiretroviral compound is a new therapeutic anti HIV option, in combination with another drug such as a NRTI or a protease inhibitor. It's heightened and sustained antiretroviral potency is due to the increased intracellular level of 3TC triphosphate, the active form of 3TC. This effect is obtained by combining 3TC, in usual doses, with a reduced dose of ddC, in the same pharmaceutical formulation. The product could be administered twice or even once daily, which is convenient, and does not increase the pill burden for the patient. The reduced ddC dosage prevents the occurrence of ddC related side effects. Other cytidine derivatives (racemic or negative enantiomers) could have the same effects as ddC and could probably be combined with 3TC, and have the same effect. On the other hand, low dose ddC may also increase the intracellular levels of other cytidine derivatives as it does for 3TC. Boosted cytidine analogue reverse transcriptase inhibitor antiretroviral compound could also be formulated in combination with another drug such as another NRTI (e.g. abacavir) or any protease inhibitor in the same capsule or tablet. This approach offers a dual anti-HIV therapy that is as efficacious as the routine triple therapy. In this way the HIV treatment cost could be significantly reduced which is imperative for resource-poor settings. This new formulation is convenient and well tolerated with no additional toxicity than that of the combining drug (NRTI or protease inhibitor) and 3TC. Moreover, this will enable a larger number of patients to benefit from the already known 3TC effects. It will also increase the 3TC effects in those organs or HIV sanctuaries with usually reduced 3TC concentrations or activity. It could be indicated in both the initial as well as in salvage HIV therapy. It could also be used for therapy optimization or simplification. Moreover, in combination with another NRTI such as abacavir, or even alone, it could be beneficial for reducing the HIV harm in resource-poor settings.
US7608253 end-capped polyethylene glycol carbamate derivatives useful as water-soluble pro-drugs; controll hydrolytic degradation of hydrogels; conjugate polymer drug for controlled release Poly(ethylene glycol) carbamate derivatives useful as water-soluble pro-drugs are disclosed. These degradable poly(ethylene glycol) carbamate derivatives also have potential applications in controlled hydrolytic degradation of hydrogels. In such degradable hydrogels, drugs may be either trapped in the gel and released by diffusion as the gel degrades, or they may be covalently bound through hydrolyzable carbamate linkages. Hydrolysis of these carbamate linkages releases the amine drug at a controllable rate as the gel degrades.
CN103585168A Medicine composition containing gemcitabine hydrochloride The invention belongs to the technical field of medicines, and discloses a medicine composition containing gemcitabine hydrochloride. The medicine composition comprises the gemcitabine hydrochloride, 95% of ethanol, a pH modifier and water for injection. The pH modifier of the medicine composition adopts sodium hydroxide; the content of sodium carbonate thereof and the content of ethanol have important effects on the quality of gemcitabine hydrochloride preparations; the pH modifier of the medicine composition adopts citric acid and disodium hydrogen phosphate; the proportional relation thereof and the content of ethanol have important effects on the quality of gemcitabine hydrochloride preparations. Through the research of stability experiments, preparations prepared by the medicine composition disclosed by the invention are less in variation of total impurities of cytosine, alpha-gemcitabine and 2'-deoxidation-2', 2'-difloxuridine.
US20120004270 Selective Androgen Receptor Modulators This invention provides compounds as described herein or pharmaceutically acceptable salte thereof, pharmaceutical compositions comprising a compound as described herein or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor using the compounds or compositions described herein, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) using the compounds and compositions described herein and processes for making compounds described herein and intermediates useful in the preparation of same.
WO2007113245A1 Thiazolyl dihydro-indazoles The invention relates to compounds of general formula (1), wherein R1 to R5 are defined as indicated in claim 1. Said compounds are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation. Also disclosed is the use of the inventive compounds for producing a medicament that has said properties.
US20110144154 Salts of 2-Substituted Quinolines The invention relates to salts of 2-substituted quinolines, the manufacturing method for same, and use of the same for the production of drugs. Said salts are advantageous in that the same can be obtained in crystalline form, which facilitates their implementation in the manufacture of pharmaceutical compositions.
US20080076792 Heterobifunctional Polymeric Bioconjugates Heterobifunctional polymeric prodrug platforms for delivering biologically active compounds, including proteins, monoclonal antibodies and the like are disclosed. One preferred compound is Methods of making and using the compounds and conjugates described herein are also provided.
US20100062087 Nutraceutical Treatments for Diabetic and Non-Diabetic Wound Healing In an embodiment of the present invention, a nutraceutical formula comprising a combination of two or more substances from the group: berry extract, chromium, zinc, trans-resveratrol, l-arginine, chlorophyll, vitamin C and aloe vera combined synergistically to reduce inflammation in mammals suffering from diabetes. In another embodiment of the present invention, a nutraceutical formula comprising a combination of two or more substances from the group: berry extract, chromium, zinc, fr-απs-resveratrol, l-arginine, chlorophyll, vitamin C and aloe vera combined synergistically to enhance wound healing in mammals suffering from diabetes. In an alternative embodiment of the present invention, a nutraceutical formula comprising a combination of two or more substances from the group: berry extract, chromium, zinc, trans-resveratrol, l-arginine, chlorophyll, vitamin C and aloe vera combined synergistically to reduce inflammation in mammals not suffering from diabetes. In another embodiment of the present invention, a nutraceutical formula comprising a combination of two or more substances from the group: berry extract, chromium, zinc, trans-resveratrol, l-arginine, chlorophyll, vitamin C and aloe vera, combined synergistically to enhance wound healing in mammals not suffering from diabetes.
US6846939 Minocycline compound substitued at 9-position by a group selected from nitro, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsufinyl, alkylsulfonyl, amino, thionitroso, arylalkynyl or carbamate, urea, and sulfonamide The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
US20100047177 treating or preventing axonal degradation in neuropathic diseases in mammals; axonopathy; administering an agent that increases AMP activated kinase (AMPK), LKB1 and CaMKK beta acitvity in diseased and/or injured neurons and supporting cells in an amount effective to decrease axonal degeneration Methods of treating or preventing axonal degradation in neuropathic diseases and neurological disorders in mammals are disclosed. The methods can comprise administering to the mammal an effective amount of an agent that acts at least in part by increasing sirtuinAMPK activity, LKB 1 activity and/or CaMKKβ activity in diseased and/or injured neurons. The methods can also comprise administering to the mammal an effective amount of an agent that acts by increasing NAD activity in diseased and/or injured neurons, alone or in combination with agents that act by other mechanisms. Also disclosed are methods of screening agents for treating a neuropathies and recombinant vectors for treating or preventing such neuropathies.
US8618104 Salts of methyl (R)-7-[3-amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-A]pyrazine-1-carboxylate The pharmaceutically acceptable salts of methyl (R)-7-[3-amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-carboxylate, their preparation methods and their use for preparing anti-diabetic medicaments are disclosed.
US20120264771 Method for Treating Androgen Receptor Positive Cancers Provided is a method of inhibiting growth of androgen receptor positive cancer cells. The method entails administering to an individual diagnosed with or suspected of having an androgen receptor positive cancer and administering to the individual a composition containing a compound that can inhibit the growth of the androgen receptor positive cancer.
EP1159756B1 Compounds for the treatment of cancer It is shown that the potency of anti-cancer drugs, here exemplified by doxorubicin, can be increased by the use of polyunsaturated fatty acid amides and in particular specific combinations of such compounds, forming complexes with doxorubicin. Further, a modified form of doxorubicin is presented.
US7378438 Asthma; side effect reduction; converting SH groups to SNO groups of N-benzylphthalimide usingHCl and NaNO2; epoxide or thioepoxid of N-benzylphthalimide; amination; 5-{2-[(1-Yloxyl-2,2,5,5-tetramethyl-pyrrolidin-3-ylmethyl)-amino]-1-S-nitroso-ethyl}-1,1,3,3-tetramethylisoindolin-2-yloxyl, hydrochloride The present invention relates to multifunctional β-agonist compounds comprising a reactive oxygen species scavenger group and a nitric oxide donor, and their use for the treatment of respiratory diseases involving airway obstruction, such as asthma and chronic bronchitis. The invention further relates to methods and devices for administering the compounds.
CN102100690B Application of flavonoids compounds in preparation of anticomplement medicaments The invention belongs to the field of Chinese pharmaceutical technology, and relates to application of flavonoids compounds(formula I) in the preparation of anticomplement medicaments. The flavonoids compounds are extracted from ethyl acetate of Sophora flavescens, and in vitro anticomplementary activity screening tests of the flavonoids compounds prove that the flavonoids compounds have quite good effect of inhibiting the classical pathway and the alternative pathway of a complement system. The CH50 of the effect of the flavonoids compounds in inhibiting the classical pathway is 0.12+/-0.02mg/mL to 0.35+/-0.03mg/mL, and the AP50 of the effect of the flavonoids compounds in inhibiting the alternative pathway is 0.45+/-0.05mg/mL. The flavonoids compounds can be furthered used for preparingthe anticomplement medicaments.
CN101912612A Dispersible tablet containing fibrate and statin drug and application thereof The invention relates to a novel dispersible tablet consisting of a certain amount of fibrate drug or pharmaceutically acceptable salts or esters or derivatives of the fibrate drug and a certain amount of statin drug or pharmaceutically acceptable salts or esters and pharmaceutically acceptable carriers of the statin drug for treating dyslipidemia of patients. Compared with the ordinary tablet or capsule, the dispersible tablet has the characteristics of rapid and even dispersion, short disintegration time, rapid drug digestion, high bioavailability, good stability and convenient taking.
EP1255870B1 5-hydroxytryptamine transporter gene polymorphisms Correlations between polymorphisms in the 5-hydroxytryptamine transporter gene are a subject's phenotypic response to treatment with 5-hydroxytryptamine ligands are described. Methods of screening subjects to aid in treatment, and methods of screening 5HT ligands, are presented
US20070244118 Cyclic Amide Derivative, and Its Production and Use The present invention provides a cyclic amide derivative useful as a drug for treating thrombosis, which is represented by the formula (I)-: wherein R1 represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent chain hydrocarbon group, a represents 0, 1, or 2, X1 represents an optionally substituted lower alkylene or an optionally substituted lower alkenylene, Y1 represents —C(O)—, —S(O)— or —S(O)2—, A represents a piperazine ring which may be further substituted or a piperidine ring which may be further substituted, X2 represents a bond or an optionally substituted lower alkylene, Y2 represents —C(O)—, —S(O)—, —S(O)2— or —C(═NR7)—, X3 represents an optionally substituted C1-4 alkylene or an optionally substituted C2-4 alkenylene, Z3 represents —N(R4)—, —O— or a bond, Z1 represents —C(R2)(R2′)—, —N(R2)—, etc., and Z2 represents —C(R3)(R3′)—, —N(R3)—, etc., or a salt thereof.
US20100099742 Sensitizing Cells for Apoptosis by Selectively Blocking Cytokines The invention refers to the use of a cytokine antagonist which modulates the expression and/or the function of a cytokine, particularly a Th2 helper cell cytokine, in a cell and causes the down-regulation of anti-apoptotic proteins in said cell through the cytokine modulation for sensitizing cells for apoptosis. In particular, the cells that can be treated with the cytokine antagonists are drug-resistant cancer cells which fail to undergo apoptosis.
US20110145970 Detection and use of low molecular-weight modulators of the cold-menthol receptor trpm8 The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
CN101627825B Novel method for extracting pectin from sweet potato dregs The invention discloses a novel method for extracting pectin from sweet potato dregs. The method comprises the following steps of: 1) preparing the sweet potato dregs into a suspension, carrying out physical screening processing on the suspension, and removing most starch to obtain dietary fibers with higher purity; 2) using amylase to carry out enzymolysis on residual small amount of starch in the dietary fibers in step 1), carrying out centrifugation, removing supernate, and collecting sediments; and 3) preparing the sediments obtained in step 2) into the suspension, adding Na2HPO4 solution into the suspension to extract the pectin, carrying out centrifugation after extracting, collecting supernatant, and carrying out concentration and drying to obtain pectin powder. The method can make the extraction ratio of the sweet potato pectin reach 95.87 percent and the purity of pectin products reach 91.28 percent (taking Xu55-2 as a material). The method has the advantages of high extraction ratio, high pectin purity, strong practicality, easy industrialization and the like. The products can be directly used as food additives or pharmaceutical excipients. The method not only can improve the comprehensive economic benefit of potato processing, but also can reduce the environmental pollution caused by accumulation of the potato dregs.
CN103755595A Hydroxamic acid derivative and application thereof The invention relates to a hydroxamic acid derivative with a structural formula (I), wherein R1, R2, R3 and L are defined in the specification of the invention. The invention further relates to application of the hydroxamic acid derivative with the structural formula (I) as a histone deacetylase (HDAC) inhibitor or/and a PARP-1 (Poly-ADP-Ribose Polymerase-1) inhibitor.
CN1566131A Small interference RNA molecule SiRNA capable of attacking human hepatitis B virus and application thereof The invention provides a small interference RNA molecule SiRNA capable of attacking human hepatitis B virus, which is double chain RNA molecule whose sequence has at least 70% of consanguinity degree with the sequence (I), wherein the antisense chain of the sequence (I) and one nucleic acid mutant has no consanguinity with the known human gene and gene expression segment. The SiRNA can be used for preparing medicament or preparation for prevention or treating hepatitis B and any diseases relating to hepatitis B viral infection.
CN1733766A Cough and phlegm removing purple bergenia element analog and its pharmaceutical composition Disclosed is a Bergenini compound having the activity of removing phlegm with a structural formula (I), wherein R1 has an ester structure, ether structure or alkyl structure, the ester structure is benzoate, ethyl cinnamate or corresponding substituted aromatic acid ester, or esters corresponding to acids having physiological activity, the ether structure is aromatic ether or esters corresponding to alcohols or phenols having physiological activity, the alkyl structure is piperazine or its derivative, R2 is H or methoxyl.
WO2013139657A1 A mixture of polar glycolipids for use in the treatment of pain and copd The present invention concerns a method for the treatment and/or prevention of pain and/or Chronic Obstructive Pulmonary Disease (COPD) comprising administering to a subject a composition comprising a polar glycolipid obtainable from cells of a cyanobacterium Oscillatoria species (CyP).
CA2537669A1 Inhibitors of nucleoside phosphorylases and nucleosidases for treating cancer Use for treating cancer of a compound of the formula (I): (see formula I)
EP1853595A1 (1,5-diphenyl-1h-pyrazol-3-yl)oxadiazole derivatives, preparation method thereof and use of same in therapeutics The invention relates to compounds having formula (I), wherein: R1 represents a heterocylic radical selected from among formula (II), R2 represents a (C1-C5)alkyl or a cyano, R3 represents a substituted or non-substituted phenyl, and R4 represents a substituted or non-substituted phenyl, as well as to the hydrates or solvates thereof.
EP1778677B1 Heterocyclic condensed compounds useful as antidiuretic agents The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.
CN101843630B Composite containing iridoid compound and application thereof The invention discloses a composite containing iridoid such as morroniside and loganin, which is used for preparing medicaments for preventing and treating neurologic demyelinating diseases. The invention discloses a method for using the composite to treat diseases relative to neurologic demyelination.
WO2012115026A1 Tomatoside a-containing composition The purpose of the present invention is to provide a composition for preventing or treating dyslipidemia and a disease related thereto such as hypercholesterolemia or hypertriglyceridemia, and one or more members selected from among a drug for preventing an increase in cholesterol level, a drug for preventing an increase in triglyceride level and a drug for preventing cholesterol accumulation in the liver. Another purpose of the present invention is to provide a method for producing the same. A drug for preventing an increase in cholesterol level, a drug for preventing an increase in triglyceride level, a drug for preventing cholesterol accumulation in the liver, and a composition for preventing or treating a disease related to dyslipidemia, said drugs and composition each containing tomatoside A or a physiologically acceptable salt thereof. A method for producing a composition containing tomatoside A or a physiologically acceptable salt thereof, said method comprising a step for extracting a material derived from tomato fruits including tomato seeds with an organic solvent as an extraction solvent, said organic solvent being used in an amount of 10 vol% or more but less than 90 vol%.
CN1911351A Foot washing medicine for treating beri-beri, foot-sweat and foot-odour, and its prepn. method A medicine in the form of foot bath powder for treating beriberi, sweating foot and smelly foot is prepared from alkaline aluminum chloride, alum and 9 Chinese-medicinal materials including flavescent sophora root, chrysanthemum flower, aloe, mint, etc. Its preparing process is also disclosed.
CN101095684A Prunol phospholipid complexes and method for preparing the same and the application thereof The invention discloses a prunol phosphatide compound, the preparation method and its application. The prunol is water insoluble and unstable, so the biological utilization rate is very low, the medical effect is reduced, and the parenteral administration is limited. The key is to increase its solubility, so the prunol phosphatide compound is needed by market. The prunol phosphatide compound comprises prunol and phosphatide, with the weight proportion being 1: 0.5-25. The product can be used to prepare various dosage forms and combined with other active components.
CN101333236A Method for preparing clitocine and applications in antineoplastic medicaments The invention provides a preparation method for cobratoxin; as raw material, fresh giant clitocybe fruitbody is frozen and dried through vacuum and then crushed; the obtained powders are dipped in alcohol; the water extract is decompressed and concentrated into liquid extract which is then extracted with ethyl acetate and concentrated into liquid extract through decompression; the liquid extract is respectively treated with silica gel column, reversed phase RP-RP-18 and RP-RP-C8 preparation columns to get the target material. The cobratoxin provided by the invention has wide broad-spectrum anti-tumor activity and has a strong growth inhibition effect on six kinds of tumors through anti-tumor activity in vitro detection; wherein, the cobratoxin has particularly prominent killing effect on HepG2 liver cancer cells, with the half of the proliferation inhibitory concentration IC50 reaching 0.24 micron; nude mice experiments show that 3mg/kg dose of cobratoxin can significantly inhibit the growth of human hepatocellular carcinoma HepG2 nude mice xenografts, with the xenograft inhibiting rate reaching 40.1% . The invention has great significance on the development of fungal resources in China and can be applied to the preparation of anti-tumor activity drugs.
WO2011129095A1 Pyridone derivative having integrase inhibitory activity The object is to provide a novel integrase inhibitor. Disclosed are a novel compound having an antiviral effect, more specifically, a pyridone derivative having an HIV integrase inhibitory activity, and a drug, in particular an anti-HIV drug, containing the same. The aforesaid compound exerts an integrase inhibitory activity and/or a cell proliferation inhibitory activity on viruses, in particular HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases and viral infections (for example, AIDS) in which integrase participates.
US20080292709 Kits for dhea and dhea-sulfate for the treatment of chronic obstructive pulmonary disease Kits for treating or preventing chronic obstructive pulmonary disease (COPD) by using as active agent a non-glucorticoid steroid, analogue thereof, such as dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEA-S), or their salts, in an amount effective for preventing or treating COPD.
CN101138562A Pharmaceutical composition containing sertraline for treating melancholia and correlating diseases The present invention discloses a medicine compound for the treatment of the depression and the related diseases, which comprise a certain amount of sertraline or the medicine salt or the solution compound, a certain amount of sulpiride or the solution compound, one kind or various kinds of medicine loading vectors or the excipient. Because of the amount of the sulpiride and the sertraline, the effect of the compound is better than the adduction of the isolate application of each medicine. The main function of the compound is treating the depression and the related diseases as well as reducing the side effects of the antidepressant.
WO2010075665A1 A formulation of silibinin with high efficiency and prolonged action and the preparation method thereof A formulation of silibinin with high efficiency and prolonged action and the preparation method thereof are disclosed. Said formulation consists of a solid dispersion of silibinin, silicon dioxide nanoparticles of silibinin, sustained-release matrix materials and release accelerator, wherein the mass ratio of the solid dispersion, nanoparticles, matrix materials and accelerator is 1: 0.5~1.25: 0.1~0.3: 0.1~03. The drug loading rate of the nanopartiles of silibinnin is 51.29-51.77%. The solid dispersion comprises silibinin, polyvidone K30, soybean phospholipid, acrylic resin IV in the mass ratio of 1: 1~3: 0.3~0.8: 0.2~0.5.
US7423175 Vanilloid receptor (VR1) antagonists; side effects reduction, oral availability; To treat urinary incontinence, urge urinary incontinence, overactive bladder, pain, and/or inflammatory diseases such as asthma and COPD; N-[2-(2-Fluorophenoxy)ethyl]-N'-(7-hydroxy-5,6,7,8-tetrahydro-1-naphthalenyl)-urea This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VR1 antagonist and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
EP1309322B1 Use of 3-benzoylphenylacetic acid derivatives for the treatment of retinal disorders The use of 3-benzolphenylacetic acids and derivatives, including nepafenac, to treat neurodegenerative retinal disorders is disclosed.
EP2727915A1 Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof The present invention provides a convenient and efficient process for the synthesis of d 2-benzo[d][1,3]dioxoles.
WO2013044608A1 Anomeric alkyl-containing phenyl c-glucoside derivative, preparation method therefor and use thereof The present invention relates to the field of drugs associated with diabetes. Specifically, the present invention relates an inhibitor of sodium-dependent glucose transporter-2 having an anomeric alkyl-containing phenyl C-glucoside structure represented by Formula I, and a preparation method for same, a pharmaceutical composition containing same and a use of same in the preparation of drugs for treating diabetes. In Formula I, R1 is selected from C1-C5 alkyl groups; R2 and R3 are each independently selected from H, OH, C1-C5 alkyl groups, F, Cl, Br, I, CN, NO2, CF3, CHF2, CH2F, OR8, SMe and cycloalkyl groups containing 3 to 5 carbon atoms, wherein R8 is selected from C1-C5 alkyl groups; R4 and R5 are each independently selected from H, C1-C5 alkyl groups and OR8, wherein R8 is selected from C1-C5 alkyl groups or cycloalkyl groups containing 3 to 5 carbon atoms; and R6 and R7 are each independently selected from H and C1-C5 alkyl groups, or R6 and R7, together with a carbon atom connected thereto, form a cycloalkyl group containing 3 to 5 carbon atoms.
US20080318984 Compounds Having Activity in Correcting Mutant-Cftr Processing and Uses Thereof The invention provides compositions, pharmaceutical preparations and methods for correcting cellular processing (e.g., folding, trafficking, or post-translational modification) of a mutant-cystic fibrosis transmembrane conductance regulator protein (e.g., ΔF508 CFTR) that are useful for the treatment of cystic fibrosis (CF). The compositions and pharmaceutical preparations of the invention may comprise one or more aminobenzothiazole-containing compounds, aminoarylthiazole-containing compounds, quinazolinylaminopyrimidinone-containing compounds, bisaminomethylbithiazole-containing compounds, or phenylaminoquino-line-containing compounds of the invention, or an analog or derivative thereof.
CN101270143B Triterpene saponin antineoplastic compound, preparing method and uses The present invention discloses a triterpenoid saponin anti-tumour compound, a preparation method and applications, and the structure of the compound is shown as (I). The present invention has the advantages that the extracted triterpenoid saponin anti-tumour compound has anti-tumour activity, and the preparation method is simple.
CN103316304A Insomnia treatment plaster An insomnia treatment plaster comprises, by weight, 6 parts of keel, 5-7 parts of magnet, 5-7 parts of mint, 6-8 parts of Radix Curcumae Aromaticae, 6-8 parts of cinnamon and 6-8 parts of Mythic Fungus. The plaster has the advantages of insomnia treatment only through plastering the plaster on the temple, use convenience, long-time effect performance, no destroy of the digestive juice to the drugs of the plaster, fast absorption, fast effectiveness, no toxic side effects to the liver, and no dependence of patients. The plaster has good curative effects on insomnia symptoms comprising difficulty falling asleep, dreaminess, festless sleep, difficulty falling asleep after waking, too early morning waking, morrow lassitude and dizziness, and the like caused by various reasons, substantially improves the insomnia degree, increases the sleep quality, prolongs the sleep time, and has an ideal insomnia treatment effect.
US20130029924 Glycosylated valproic acid analogs and uses thereof Glycosylated valproic acid and its analogs are provided. In some embodiments, the glycosylated valproic acid and its analogs have improved solubility and are ideal for drug delivery to treat a variety of diseases.
CN101270152B Peptide medicament series for accelerating medulla hematopoiesis cell proliferation The present invention provides peptide drug series that can promote the proliferation of marrow hematopoietic cells. The main amino acid sequence of the short peptide fragments, analogs, derivants and variants of the short peptide of the peptide drug series is larger than or equal to 70 percent equal to and larger than or equal to 90 percent similar to the main amino acid sequence of the short peptide. The short peptide, nucleotides, short peptide fragments, short peptide analogs, short peptide derivants and short peptide variants are used for the preparation of drugs for treating manifold marrow hematopoietic cell defection diseases, congenital anaemia, aplastic anemia and various hemorrhagic anemia diseases and can be applied to the bone marrow transplantation of leukemia patients, etc., that is, the peptide drug of the present invention can treat pancytopenia caused by hemopoietic stem cell defects.
CN103230377A Antibiosis fishing medicament processing method The invention discloses an antibiosis fishing medicament processing method, and has the advantage that the antibiosis fishing medicament prepared by the method contains a macro-molecule system of starch/chitosan/gelatin, and the system can form a macro-molecule interpenetrating network structure, thereby the antibiosis fishing pills prepared by the method have an obviously improved stability in seawater and are not easy to be dispersed; in addition, gelatin, chitosan and starch three compositions belong to natural large molecules which are friendly to environment, and in the preparation process, water is used as a solvent for starch dextrinization at first, and then another two compositions are gradually added; according to detection, the antibiosis fishing medicament obtained by the processing method has the advantages of uniform internal porosity structure, large porosity, uniformly distributed apertures, good connectivity between apertures, thereby the fishing medicament can be uniformly distributed in the carrier.
US20050148777 (2R)-6-chloro-7-isobutyl-2-(trifluoromethyl)-2H-chromene-3-carboxylic acid; cyclooxygenase-2 mediated disorders The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula 1 Wherein Z, X, R1, R 2, R3, and R4 are as described in the specification.
US20080070938 HMG-CoA reductase inhibitor and pyridoxine, pyridoxal, or pyridoxamine; combination therapy; pravastatin, simvastatin, atorvastatin A method of mitigating blood lipid levels or reducing high blood homocysteine levels administering in amounts effective for mitigating blood lipid levels or reducing high blood homocysteine levels, an HMG-CoA reductase inhibitor and a pyridoxine derivative. The pyridoxine derivative is one or more of pyridoxine, pyridoxal, pyridoxamine, and their pharmacologically acceptable salts.
US6884412 Dectection of and methods and composition for prevention and/or treatment of papillomatous digital dermatitis The present invention relates to the use of Serpens spp. bacteria or bacterin in compositions, such vaccines, and methods for the detection, prevention and/or treatment of Papillomatous Digital Dermatitis in ruminants. The present invention also provides biologically pure Serpens spp. strain HBL-112, and biologically pure Serpens spp. strain HBL-112 bacterin.
CA2324418C Novel opiate compounds, methods of making and methods of use Disclosed are a class of nitrogen-containing heterocyclic compounds having the general formula: (see formula I) wherein R1, R2 and R3 are defined herein and pharmaceutically acceptable salts thereof. The compounds bind to opioid receptors and can be used to treat a variety of disease states which involve the opioid receptors.
CN101095953A Treating cancer through attracting effect T cell and loss regulating T cell The invention relates to the utilization of regulative T cell deterioration agent for medicine preparation. Said medicine treats or prevents tumor (especially cancer)by deteriorating the regulative T cell for patient (including animal, mammalian, especially human being). One example for regulative T cell deterioration agent is anti-CD4+ antibody, such as CD4+CD25+ antibody and IL2-toxin. The invention also relates to regulative T cell deterioration agent - containing medical compound and method of using regulative T cell deterioration agent or said compound to treat cancer.
CN101019905A Medicine composition containing tribulus fruit furostanol saponin and its application The present invention discloses one kind of medicine composition containing tribulus fruit furostanol saponin. The medicine composition has furostanol saponin extracted from tribulus fruit as main component, and the tribulus fruit furostanol saponin has weak hemolysis and high water solubility. The medicine composition is prepared into injection for intravenous injection to treat ischemic cardiacand cerebral vascular diseases, and has high effect and high safety.
CA2717537A1 2-trifluoromethylnicotinamide derivatives as hdl-cholesterol raising agents The present invention relates to compounds of the formula (I) wherein R1 to R8 are as defined in the description and claims, for the preparation of medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL--cholesterol raising agents, such as preferably dyslipidemia.
CA2284976C Process for preparing single enantiomer narwedine A process for the preparation of substantially single enantiomer (-)-narwedine comprises seeding a solution of racemic narwedine dissolved in a solvent with substantially single enantiomer (-)-narwedine, provided that if an added amine base is present the ratio solvent: added amine base is greater than 15:1.
US20110052672 Treatments of disease or disorders using nanoparticles for focused hyperthermia to increase therapy efficacy Methods are provided for the treatment of diseases and disorders using systematically-introduced nanoparticles to create a focused localized hyperthermia in a target area to enhance the effect of additional treatment therapies such as ionizing radiation. Advantages include an enhancement of the therapeutic effect of other therapies by increasing perfusion or reducing hypoxia in the treatment area, further, the methods herein may also result in the disruption of the vasculature, which provide further impetus for such treatments, singly and in combination with conventional therapies such as chemotherapy and radiation therapy. Methods for treating a target area may comprise systemically introducing nanoparticles into an organism; allowing the nanoparticles to preferentially accumulate in the target area, applying an external energy where the nanoparticles are adapted to transduce at least a portion of the external energy into a heal energy so as to create a focused localized hyperthermia; and applying a subsequent additional therapy.
US20080031948 admixed with hydroxyalkylcellulose, polyvinylacetate, blends of polyvinylacetate and polyvinylpyrrolidone, a vinylpyrrolidone copolymer and polyethylene oxide; enteric coating Sustained-release bupropion hydrochloride pharmaceutical tablets and combination sustained-release bupropion hydrochloride/mecamylamine hydrochloride pharmaceutical tablets are obtained by granulating the bupropion hydrochloride with a hydroxyalkylcelluose, and blending the resulting granules within an extragranular phase composed of a particulate material that provides a sustained-release matrix, and compressing the blend into a tablet form, which then is coated, with a means to provide delayed release, such as with an enteric coating composition. The mecamylamine hydrochloride can be contained in a second granule comprising a hydroxyalkylcellulose.
US20120064133 Multiparticulate Controlled-Release Selective Serotonin Reuptake Inhibitor Formulations Multiparticulate controlled-release selective serotonin reuptake inhibitor (SSRI) formulations for oral administration, which comprise subunits of a SSRI or a pharmaceutically acceptable salt thereof which are not coated with a rate-controlling polymer, are provided. Methods for preparation and use of these formulations are also provided.
CN1843335A Quisnon dispersion tablet The invention provides a dispersible tablet preparation containing antiseptic Prulifloxacin, wherein the constituents of the preparation include Prulifloxacin, lactose, crystalline cellulose, sodium carboxymethylstarch, polyvidone and talcum powder.
EP2557082A1 Cephem compound having catechol group A compound of the formula: wherein X is -N=, -CH=, or the like; W is -CH2- or the like; U is -S- or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; R3 is hydrogen or the like; each R4 is independently hydrogen, halogen, or the like; m is an integer from 0 to 2; Q is a single bond, or the like; G is -C(=O)-, or the like; D is a single bond, -NH-, or the like; and E is a cyclic quaternary ammonium group, or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.
US20050281824 Methods of using IMXP-888 and IMXP-888 antagonists The invention relates to the discovery that IMXP-888, a protein with homology to the FGF receptor family, is a proinflammatory cytokine. The invention encompasses therapeutic compositions of IMXP-888 polypeptides and antagonists, methods of use thereof, and screening methods.
CN1648136A Companumoea root polyose, derivative and its preparing method and use Companumoea polyose is obtained through extracting coarse polyose from companumoea root and chromatographic purification and refining. Bioactivity test shows that companumoea polyose has obvious effects of promoting nerve cell growth and differentiation and repairing damaged nerve cell similar to nerve growth factor. Therefore, companumoea polyose may be used in medicine for preventing and treating senile dementia, learning memory disorder, children's hypophrenosis, apoplexy and other diseases, and health food for improving memory and protecting brain.
US20100196473 Pharmaceutical Composition Containing 6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol with Delayed Active Ingredient Release Pharmaceutical compositions with delayed release which contains 6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol or a pharmaceutically acceptable salt thereof in a matrix with delayed active ingredient release, wherein the matrix contains 1 to 80 wt. % of one or more hydrophilic or hydrophobic polymers as pharmaceutically acceptable matrix formers and exhibits the following in vitro release rate: 3-35 wt. % (relative to 100 wt. % of active ingredient) of 6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol released after 0.5 hours, 5-50 wt. % after 1 hour, 10-75 wt. % after 2 hours, 15-82 wt. % after 3 hours, 30-97 wt. % after 6 hours, more than 50 wt. % after 12 hours, more than 70 wt. % after 18 hours, and more than 80 wt. % after 24 hours.
CN102898370A Cis-atracurium besilate for injection The invention relates to the field of pharmaceutical chemistry, and practically provides cis-atracurium besilate for injection and a preparation method thereof. The method disclosed by the invention is stable and reliable and small in pollution to environment and the product impurity content is low.
US20100285064 Adjuvant composition for vaccine The present invention provides a Withania somnifera fraction rich in withanolides and a vaccine comprising a “Withania somnifera fraction” as an adjuvant.
WO2012129066A2 New targets for treatment of er stress The embodiments of the invention provide for genetic, chemical or dietary interventions that modulate hepatic phospholipid synthesis and/or endoplasmic reticulum (ER) calcium homeostasis function. More specifically, the present invention addresses modulation of the lipid composition of the hepatic stressed ER and/or improvement of the hepatic ER calcium metabolism to reduce ER stress and thus treat type 2 diabetes, fatty liver disease, atherosclerosis, inflammation, and/or dislipidemia.
US7153886 Method for treatment of peripheral inflammation of a loop ileal artificial anus The present invention provides a novel agent for prophylaxis or treatment of inflammatory bowel diseases for oral administration or intra-intestinal infusion, which comprises as an active ingredient a compound of the formula (I): or a pharmaceutically acceptable salt thereof; a use of said active ingredient in preparation of an agent for prophylaxis or treatment of inflammatory bowel diseases; and a method for prophylaxis or treatment of inflammatory bowel diseases.
US8128964 Transdermal pharmaceutical delivery composition A pharmaceutically delivery system is described comprising a pharmaceutically active agent and acidified nitrite as an agent to produce local production of nitric oxide at the skin surface. The dosage form may be in any pharmaceutically acceptable carrier means and comprises an acidifying agent adapted to reduce the pH at the environment. In one embodiment, a barrier consisting of a membrane allows diffusions of the anaesthetic and nitrite ions while preventing direct contact of the skin and acidifying agent.
US7098228 Indolyl derivatives The present invention provides compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4, A and n have the significance given in the specification. The compounds or their salts may be administered to a patient for treating non-insulin dependent diabetes mellitus.
CN1615884A Use of lycopene in producing medicine The present invention relates to new use of lycopene. Lycopene can remit the ischemic necrosis of hippocampal pyramidal cell, prevent neuronal degeneration damage and increase HP positive cells in CA1 region obviously. The strengthening of HP protein can promote release of iron from inside the cell to outside the cell and reduce intracellular iron content to reduce cell damage caused by oxidative stress. Therefore, the present invention can prevent ischemic cerebral damage and may be used in preparing medicine for preventing and treating ischemic cerebral damage.
WO2006018657A1 Hdac inhibitors and methods of use thereof According to the present invention there is provided the use of a histone deacetylase inhibitor in the manufacture of a medicament for the treatment of a disease associated with the destruction of connective tissue mediated by metalloproteinases.
CN103356565A Application of Sarcaboside B in preparation of drug for promoting insulin secretion The invention belongs to the pharmaceutical field and discloses application of Sarcaboside B in preparation of a drug for promoting insulin secretion. The application of Sarcaboside B in preparation of the drug for promoting insulin secretionis is disclosed by the invention for the first time. As the skeleton type is brand new and Sarcaboside B has unexpectedly strong activity for promoting insulin secretion, the possibility that any enlightenments are given by other compounds does not exist. Sarcaboside B has prominent substantive features and has remarkable progress when being used for preventing and treating diabetes mellitus II.
WO2007146323A3 Substituted cyanopyridines as protein kinase inhibitors The present teachings provide compounds of formula (I) and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula (I), and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula (I) to a mammal including a human.
CN1887295A Medicine for promoting healing of wound The present invention relates to medicine for promoting healing of wound, and the medicine has 200-300 mesh egg shell carbon powder as main component and connects certain amount of streptomycin sulfate powder, calcium pantothenate powder, niacinamide powder, vitamin C powder, vitamin B6 powder and vitamin B2 powder. The medicine is grayish powder prepared through mixing the said components and grinding. The medicine is used in treating various kinds of traumatic wound, external infection, small area light burns and scalds, ulcer, chronic rhinitis and other common diseases.
CN102764328A Externally-applied medicinal liquid for curing vitiligo The invention discloses an externally-applied medicinal liquid for curing vitiligo. The externally-applied medicinal liquid is formed by following components in part by weight: 20 to 40 parts of galenite, 5 to 15 parts of calomel, 10 to 20 parts of golden cypress, 20 to 25 parts of tribulus terrestris, 10 to 15 parts of black bean peel, 5 to 7 parts of Chinese angelica, 20 to 25 parts of fructus psoraleae, 5 to 8 parts of borneol, 15 to 20 parts of radix angelicae, 25 to 30 parts of cortex dictamni, 20 to 25 parts of cucumber pedicel, 12 to 15 parts of cacumen biotae, 10 to 12 parts of three-season red leaves and 1600 parts of mature vinegar. The externally-applied medicinal liquid can promote blood circulation to remove meridian obstruction and dispel the wind and take off vitiligo, and has good curing effect and no any side effects.
CN102772388A Method for preparing flupirtine maleate capsule The invention discloses a method for preparing a flupirtine maleate capsule. The method comprises the following steps of: (A) weighting calcium hydrophosphate, crosslinking polyvinylpyrrolidone, lauryl sodium sulfate, magnesium stearate and superfine silica powder according to a formula and sieving through a sieve of 100 meshes; (B) performing superfine grinding on a flupirtine maleate raw material according to the formula until the particle size is 10 to 25 mu m, and uniformly mixing the treated flupirtine maleate raw material with the auxiliary materials in the step (A) according to an equivalent adding method; (C) granulating 50 percent of ethanol solution with the volume of 80 to 100 ml serving as an adhesive preparation soft material after sieving through a sieve of 20 meshes; (D) drying the wet particles prepared in the step (C) at the temperature of 55 to 65 DEG C for 2 to 4 hours, and arranging the particles after sieving through the sieve of 20 meshes; and (E) uniformly mixing the magnesium stearate and the superfine silica powder according to the formula, and filling to obtain the flupirtine maleate capsule. The method is ingenious in concept and simple in flow; the flupirtine maleate capsule is high in blood concentration, small in medicine amount and high in bioavailability; and the pain treating effect is obvious.
CN102552125A Injection composition containing oxiracetam and preparation method and application thereof The invention provides an injection composition containing oxiracetam and a preparation method and an application thereof. The composition contains sodium hydroxide. The invention further provides a preparation method and an application of the medicinal composition. The composition is mainly used for improving memory and the memory learning function of a mentally retarded patient, and is suitablefor memory and amentia caused by symptoms such as mild or moderate vascular dementia, senile dementia, brain trauma and the like, or is taken as an auxiliary treatment medicament.
US20110294763 Transdermal delivery of dicolfenac, carbamazepine and benzydamine The invention discloses solutions of diclofenac, carbamazepine and benzydamine, at therapeutically desirable concentrations and the solutions stable for extended periods of time at room temperature.
WO2014163520A1 Preparation for treating proctological, urological and gynaecological diseases The invention relates to medicine and concerns a combined preparation for treating diseases of the rectum and female genitalia (erosion, colpitis, condylomas, cysts, endometriosis, myomas, fibroids, polyps of various localisation, lesions resulting from surgical interventions), which can also be used in antineoplastic combination therapy. The technical result achieved by carrying out the claimed invention is to enhance the therapeutic effect of the drug dosage form presented as a suppository comprising effective active substances having anti-inflammatory, anti-microbial, local anaesthetic, wound healing, adaptogenic and anti-tumour properties for treating proctological, urological and gynaecological diseases. Said technical result is achieved in that the combined preparation "Gemodan" for treating proctological, urological and gynaecological diseases in the suppository form comprises diosmin as an active substance, and glycerides of fatty acids as a pharmaceutically acceptable suppository base, and further comprises an oil extract of a medicinal mud from Lake Tambukan and kamellin as bioactive active substances, wherein the total suppository weight is from 1.0 to 3.0 g and the component ratio is, in g: diosmin 0.05-0.2, oil extract of medicinal mud from Lake Tambukan 0.1-0.3, camellin (green tea extract) 0.05-0.2, suppository base - glycerides of fatty acids (the remainder).
CN103159695A Thiazole compound capable of restraining human immunodeficiency virus (HIV) replication and effective against drug-resistant HIV virus strains and preparation method and purpose thereof The invention provides a 2,4,5-tri-substituted thiazole compound which is in a general formula I and can serve as a human immunodeficiency virus (HIV) replication inhibitor, and all possible isomers or prodrug or medicinal salt or solvate or aquo-complex of the 2,4,5-tri-substituted thiazole compound, and further provides a preparation method for the compound in the general formula I as well as a medical composition of the compound in the general formula I, and the purpose of the compound in the medicine preparation process. The medicine is used for treating and/or preventing diseases caused by HIV infection.
CA2791805A1 Use of meloxicam for the long-term treatment of musculoskeletal disorders in cats The invention is directed to the use of a formulation comprising meloxicam or a pharmacologically acceptable meloxicam salt of an organic or inorganic base thereof for the long-term treatment of musculoskeletal disorders in cats. No negative effects on renal function occur following a treatment from 10 to 20 months or more.
CN103735501A CS/GP/MAX (Methotrexate-loaded Chitosan-based Thermosensitive Hydrogel) and application thereof The invention provides MTX subcutaneous sustained-release injection CS/GP/MAX (Methotrexate-loaded Chitosan-based Thermosensitive Hydrogel). Every liter of aqueous solution of the CS/GP/MAX contains 16 to 22 grams of chitosan, 0.05 to 0.1 mole of acetic acid, 70 to 150 grams of beta-glycerophosphate, 0.1 to 0.12 mole of methotrexate, 0.1 to 0.12 mole of a solubilizer and 5 to 50 grams of an isoosmotic adjusting agent and pH modifier. The CS/GP/MAX has stable properties and controllable quality, and the external properties, tgel (the time of gelation), eta, pH value, content and preliminary stability of the CS/GP/MAX meet requirements on thermosensitive hydrogel; 70 percent of drugs of the CS/GP/MAX in a PBS (Phosphate Buffer Solution) are released within 5 days under the condition of 37 DEG C; compared with those of MTX injection, the Cmax (Maximum Plasma Drug Concentration) is reduced by 82 percent, the AUC0-t (area under the plasma concentration time curve from time 0 to t hours) is enlarged by 2.37 times, and the t0.02muM (the length of time the MTX concentration-time curve remained above 0.02 muM in one week) is prolonged by 12.93 times after the CS/GP/MAX is subcutaneously injected to the back of a rabbit; by the CS/GP/MAX, adverse effects can be reduced, and curative effects can be improved.
US20100316734 Methods of thermograph-guided medical treatment Methods and systems for treatment based on thermographic images of a patient to detect temperature patterns indicative of an evolving disease process. Guided by the thermographic image obtained, a treatment means can be positioned on the skin of the imaged body part. The treatment means comprises a medicament that reduces risk factor(s) associated with the progression of the evolving disease process.
WO2005063236A1 Intranasal formulation of rotigotine This invention pertains to a liquid intranasal pharmaceutical formulation comprising a pharmaceutically acceptable acid addition salt of rotigotine and α-cyclodextrin, preferably in the form of a buffered aqueous solution having a viscosity of 0.5 - 1.5 mm2/s
CN101647800B Combination of cefuroxime sodium The invention relates to a combination of cefuroxime sodium, which is characterized in that the combination is combination of the cefuroxime sodium and arginine. A preparation method comprises the following steps: under the bacteria-free environment, bacteria-free raw materials of the cefuroxime sodium and the arginine are weighed according to a prescription proportion to be uniformly mixed, and then the mixture is separately packed. The combination solves problems that the active components of cefuroxime sodium is not insoluble in water, the original medicament of cefuroxime sodium is unstable, and products are unqualified caused by easy standard exceeding of colors, and can be preserved, stored and transported under the shady and cool condition.
CN101991559A Stable Agomelatine capsule medicine composition The invention discloses a stable Agomelatine capsule medicine composition which is characterized in that 1000 capsules comprise the following components of 15-30g of Agomelatine, 70-140g of mannitol, 0.5-1g of superfine silica powder and a proper amount of 10 percent pre-gelatinized starch. The invention also relates to a preparation method of an Agomelatine capsule. The Agomelatine capsule prepared by adopting the formula and the preparation method provided in the invention has the advantages of good flowability, good dissolution rate, small content uniformity, high bioavailability and good treatment effect.
CA2769623A1 Treatment of crohn's disease with laquinimod This application provides for a method of treating a subject suffering from Crohn's disease, the method comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This application provides for use of laquinimod in the manufacture of a medicament for treating a subject suffering from Crohn's disease. This application also provides for a pharmaceutical composition comprising laquinimod for use in treating a subject suffering from Crohn's disease.
CN102824356A Baicalin nano crystal suspension, nano crystal dry powder and methods for preparing baicalin nano crystal suspension and nano crystal dry powder The invention relates to a baicalin nano crystal suspension, a nano crystal dry powder and methods for preparing the baicalin nano crystal suspension and the nano crystal dry powder, which are used for effectively solving the problems that baicalin has bad water solubility, low oral bioavailability and common injections hardly achieve high drug-loading rate and a targeting function. A baicalin nano crystal intermediate is characterized by consisting of 1 part by weight of baicalin, 0.01-10 parts by weight of stabilizer and 0-30 parts by weight of filling protective. The baicalin nano crystal intermediate can be a nano crystal suspension and the dry power of the nano crystal suspension, which are prepared by the following steps: 1, preparing a nano primary suspension by using a dispersion method; 2, preparing the nano crystal suspension by a grain size reducing method which can be a high-pressure homogenization method or an ultrasound grinding method; and 3, preparing nano crystal dry powder by using a freeze-drying method and a spray drying method.
CA2602442A1 Ep2 receptor agonists for treating glaucoma The present invention provides novel compounds represented by the formula wherein R is as defined in the specification and wherein said compounds are useful for treating ocular hypertension and/or providing neuroprotection to the eye of a mammal.
CN101019839A Application of beta-elemene in preparing hypoglycemic medicine The present invention discloses the new use of beta-elemene in preparing hypoglycemic medicine. Experiments prove the obvious hypoglycemic effect of beta-elemene up to 57 %, so that beta-elemene may be used as the active component in preparing hypoglycemic medicine. The hypoglycemic medicine has the advantages of obvious hypoglycemic effect, high safety, convenient use and low cost. The present invention provides one new way of lowering blood sugar and has wide medicine application foreground.
EP1185268B1 The therapeutic use of d-threo-methylphenidate for the treatment of attention-deficit hyperactivity disorder d-threo-methylphenidate is useful for the treatment of, e.g. attention-deficit hyperactivity disorder in a patient who does not respond to treatment with racemic methylphenidate.
CN103690514A Timed controlled-release amlodipine capsule and preparation method thereof The invention relates to a timed controlled-release amlodipine capsule and a preparation method thereof. The amlodipine capsule comprises an impervious capsule body, a floating aid, amlodipine powder or tablet, a time-lag embolism tablet and a gastric soluble capsule cap, wherein the impervious capsule body has a structure with one closed end and one opened end and is filled with the floating aid and the amlodipine powder or tablet, the time-lag embolism tablet is encapsulated at an opening of the impervious capsule body, and the gastric soluble capsule cap is used for covering the impervious capsule body. The timed controlled-release amlodipine capsule can lastingly float in gastric juice for a set time and then quickly release active pharmaceutical ingredients, the seepage phenomenon is not caused within the lag time, the active pharmaceutical ingredients-amlodipine are released after a certain time lag, the lag time and the time-lag reproducibility are effectively controlled by the components and the component ratio of the time-lag embolism tablet, and a drug release mechanism is that the time lag is controlled by dissolving the time-lag embolism tablet. Therefore, a patient can conveniently take medicines for treatment and the compliance of the patient with the treatment is improved.
WO2014094528A1 Compounds and methods for the treatment of cd20 positive diseases Disclosed herein are anti-CD20 antibody conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods related to the preparation and uses of such antibody drug conjugates to treat CD20 positive cells in cancers are provided.
EP1140830B1 Arylpiperidine and aryl-1,2,5,6-tetrahydropyridine amide derivatives having 5ht1a receptor activity Compounds of formula (I) wherein R1, R2, R3, R4, X and n are defined in specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other related conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and Alzheimer's disease.
US7157463 Substituted piperidines/piperazines as melanocortin receptor agonists The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
CN103265594A Garcinia acid amide derivative and preparation method thereof and purpose The invention relates to garcinia acid amide derivative and preparation method thereof and purpose, and the structural formula of the derivative is shown as formula (I); The preparation method comprises the following steps: garcinia acid and nucleoside medicament or salt nucleoside of nucleoside medicament melted in an inertia solvent under room temperature; then a catalyzed condensation reagent is added for reaction for 3 to 5 hours by blending at the temperature between 40 and 60 DEG C; and garcinia acid amide derivative is obtained after washing, drying, distillation andn column chromatography. The derivative of the present invention can be used for used to prepare compositions, antineoplastic drugs, antimycotics drugs or anti-angiogenic drugs generation medicament or be used with other anticancer active components. The compound of the present invention not only displays better activity to a plurality of tumor cells, shows good targeting to tumor cells, which makes a good foundation for novel medicament exploitation.
CN1582160A Novel herbal chemical composition for treatment of cancer The present invention relate to a novel synergistic composition of lignans exhibiting anticancer activities for breast, cervix, neuroblastoma, colon, liver, lung, mouth, mouth, ovary and prostate cancer obtained from the plant extract of Cedrus deodra, said composition comprising of (-)-matairesinol in the range of 9 to 13 % by weight, (-)-wikstromol in the range of 75to 79 % by weight, Dibenzylbutyrolactol in the range of 7 to 11 % by weight, and Unidentified material in the range of 2.6 to 3% by weight; further, the synergistic composition of lignan is used in combination with pharmaceutically acceptable carriers for inhibiting growth of various human cancer cell lines selected from breast, cervix, neuroblastoma, colon, liver, lung, mouth, ovary and prostate tissues.
WO2009007399A1 New compounds as hsp90 inhibitors The invention provides novel compounds of formula (I) wherein: one of the a, b, c or d members is a nitrogen atom and the remaining members are carbon atoms; and R3 is a radical selected from the group consisting of: -S-R14 and -CH2-R15.The compounds of formula (I) are useful for treating diseases mediated by a heat shock protein 90 (Hsp 90).
CN101328177B Nitrogen heterocyclic ring vinyl substituted sulfhydryl heterocycle carbpenem compounds The invention belongs to the medicine technical field, in particular relating to a N heterocyclic vinyl-substituted sulfhydryl heterocyclic carbopenem compound as shown in a general formula (I), a salt thereof acceptable in pharmacology, an easily hydrolyzed ester thereof, an isomer thereof, a hydrate thereof and a hydrate of the ester or the salt thereof, wherein R<1>, R<2>, R<3>, R<4>, X, Y andn are defined in a specification. The invention also relates to a preparation method of the compounds, a medicine combination containing the compounds and an application of the compounds in preparingmedicines used to treat and/or prevent infectious diseases.
US20080153867 Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction; -chloro-N-{[3-(4-chlorophenyl)-4-phenyl-4,5-dihydro-1H-pyrazolyl]-[7-(1,2,3,4-tetrahydroacridin-9-ylamino)heptylamino]methylene}benzene-sulfonamide Embodiments of this invention relate to compounds having a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition is a compound of formula (1) wherein the symbols have the meanings given in the specification.
EP2164856A1 Processes related to making capecitabine An intermediate (2) useful in making capecitabine can be formed without the use, or presence, of a silylation agent. formula (I):
CN103520141A Application of compound in preparation of medicine for treating ileocecum cancer The invention discloses the application of a compound, Asperterpenols A, in preparation of medicine for treating the ileocecum cancer and belongs to the technical field of new applications of the medicine. According to the application of the compound in the preparation of the medicine for treating the ileocecum cancer, it is proved that the Asperterpenols A has an obvious inhibiting effect on the growth of human ileocecum cancer cell strains such as HCT-8 through in-vitro MTT antineoplastic activity evaluation, so that the Asperterpenols A can be used for preparing the medicine for treating the ileocecum cancer and the development and application prospect is good. The application of the Asperterpenols A in the preparation of the medicine for treating the ileocecum cancer is disclosed for the first time, the inhibitory activity of the Asperterpenols A to ileocecum cancer cells is high, and obvious advance is achieved.
WO2013103632A1 Double-stranded rna compounds to casp2 and uses thereof The present disclosure relates to methods of treating a patient suffering from or at risk of developing an ocular disease, disorder or injury, and includes treatment regimens using a double-stranded RNA compound that down-regulates CASP2 expression, or a pharmaceutically acceptable salt thereof.
EP2394993A2 Novel 2,6-substituted-3-nitropyridine derivative, method for preparing same, and pharmaceutical composition including same The present invention relates to a novel 2,6-substituted-3-nitropyridine derivative compound, a method for preparing the same, and a pharmaceutical composition including the same for prevention and treatment of osteoporosis. The 2,6-substituted-3-nitropyridine derivative compound of the present invention increases osteoblast activity and effectively inhibits the differentiation of osteoclasts, and thus can be usefully used for the prevention and treatment of osteoporosis.
EP2682462A1 (nucleic acid)-polysaccharide complex An object of the present invention is to provide a highly stable nucleic acid-polysaccharide complex of an siRNA and schizophyllan. A nucleic acid-polysaccharide complex is formed by adding polydeoxyadenine in which at least part of the phosphodiester link portion is phosphorothioated to an siRNA and allowing the siRNA and schizophyllan to form a complex.
WO2008094476A1 Substituted pyrano [2, 3 - b] pyridine derivatives as cannabinoid -1 receptor modulators Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.
EP2675276A1 PERIPHERIALLY ACTING µ OPIOID ANTAGONISTS The present invention relates to a novel functional peripherally-acting μ opioid receptor antagonist of Formula I: The novel compounds of the present invention have reduced oral bioavailability without compromising opiate-induced analgesia in the CNS. The compounds of the present invention are further efficacious at low doses and are useful in treating gastrointestinal conditions associated with opioid analgesic therapy.
US20130274255 Heterocyclic pyrazole compounds, method for preparing the same and use thereof The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.
WO2008044261A1 Use of amiodarone and amiodarone analogues as antiviral agents The present invention regards the use of amiodarone, and structurally related compounds, as antivirals. Amiodarone, which is widely used to treat cardiac arrhythmias, inhibits the spreading in vitro of the coronavirus responsible of the Severe Acute Respiratory Syndrome (SARS) by acting after the delivery of the viral genome into the cytoplasm. The antiviral effect of amiodarone appears to be related to changes in the host cell, rather than to a direct effect on the SARS coronavirus and starts at concentrations close to those reached in patients treated for arrhythmias. Although the fine mechanism of the antiviral activity remains to be clarified, pharmaceutical preparations containing amiodarone or structurally related compounds could be used for the treatment or the prevention of infections by the SARS coronavirus or viruses having similar strategies of infection.
CN101347620A Medicament composition and use thereof in preparing medicament for treating glaucoma The invention relates to a pharmaceutical composition, in particular to a pharmaceutical composition for the treatment of glaucoma. The pharmaceutical composition for the treatment of glaucoma consists of one or a plurality of accessories and active ingredients pharmaceutically acceptable. The composition is characterized in that the active ingredients of the pharmaceutical composition are one or a plurality of prostaglandin and one or a plurality of glucocorticoids.
CA2786834A1 1-(5-tert-butyl-2-phenyl-2h-pyrazol-3-yl)-3-[2-fluoro-4-(1-methyl-2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridin-7-yloxy)-phenyl]-urea and related compounds and their use in therapy The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (I) (for convenience, collectively referred to herein as "IP compounds"), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS ("mutant RAS cancer"). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.
US7629338 for treating migraine, headaches; N-[(4S)-3-Methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-inden]-5'-yl]-2-((6+-)-2-oxo-6-phenylpiperidin-1-yl)acetamide Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
US8183369 4- [3- (4-cyclopropanecarbonyl-piperazine-I-carbonyl) -4 -fluoro-benzyl] -2H-phthalaz in-1-one 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form L, methods of obtaining form L, pharmaceutical compositions comprising Form L and methods of using Form L and compositions comprising Form L.
CN101703606A Oral liquid for preventing diseases and epidemics and production method The invention discloses an oral liquid for preventing diseases and epidemics and a production method. The oral liquid comprises the following raw materials: rhizoma atractylodis, Chinese mugwort, Chinese arborvitae twig, pricklyash peel, peach seed, mint, purple perilla, honeysuckle flower, platycodon root, dark plum fruit, unripe liquoric root, vitamin C and honey. The production method produces the oral liquid according to the components and the technique.
CN102369001A Pharmaceutical formulation comprising one or more fumaric acid esters in an erosion matrix A pharmaceutical formulation comprising an erosion matrix comprising one or more fumaric acid esters as well as one or more rate-controlling agents, wherein erosion of said erosion matrix permits controlled release of said fumaric acid ester(s).
EP2511272A1 Synthetic analogues of abscisic acid with anti-inflammatory and insulin release stimulation effects on human cells Compound of formula (I) as drug, having abscisic acid antagonist activity and insulin release stimulating activity, in particular for treatment of inflammatory pathologies of type 2 diabetes. Compound of formula (I) wherein R is selected from hydrogen e =O groups, R1 is selected from -H e -OH, R2 is selected from groups having one of following structural formulae (II), (III): wherein X is selected from -OH, optionally substituted alkylamino-, arylamino-, alkylarylamino- or arylalkylamino-, alkoxy-, aryloxy-, alkylaryloxy- or arylalkoxy- groups, with said groups having from one to eight carbon atoms, with the alkyl chains of such groups being optionally branched, containing unsaturations or forming rings, said groups optionally containing atoms or functionalities different from C, salts of said compound or pharmaceutically acceptable precursors thereof, metabolites, hydrates or solvates thereof, for use as a drug.
CN103142569A 2, 6-diisopropyl benzoic acid and application of 2, 6-diisopropyl benzoic acid derivative serving as neuroprotective agent The invention discloses 2, 6-diisopropyl benzoic acid and the application of 2, 6-diisopropyl benzoic acid derivative serving as a neuroprotective agent, specifically the application of the compound in the preparation of neuroprotective medicines. In the compound, R is carboxyl, hydroxymethyl, carboxymethyl or hydroxyethyl. The compound disclosed by the invention has a good protective effect on glutamic acid induced neuron damage.
EP0854870B1 Substituted imidazoles having anti-cancer and cytokine inhibitory activity Compounds represented by formula (I), are disclosed. AR represents an aromatic group containing 6-10 atoms; and (a) represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional N atoms and 0-1 O or S atom. A pharmaceutical composition is also included. Methods of treating cancer and cytokine mediated diseases are also included.
US20110091412 Mutant interleukin-2 (il-2) polypeptides The present invention relates to mutant IL-2 polypeptides that act as receptor antagonists. The mutant IL-2 polypeptides bind CD 25 but do not activate the IL-2 receptor. Also provided are methods of using the mutant IL-2 polypeptides, for example, to treat a patient who has cancer or a viral infection. The mutant polypeptides can also be used in various delivery systems.
EP1609473A1 Use of acetyl-d-aminoglycosamine in treatment of local lesions and systematic symptoms related to infections of virus or bacteria The present invention discloses a use of N-acetyl-D-glucosamine or pharmaceutically acceptable salts thereof in the manufacture of a medicament for treating local lesions or systematic symptoms caused by infections of virus or bacteria. A parenteral preparation comprising N-acetyl-D-glucosamine or pharmaceutically acceptable salts thereof as active component is capable of controlling systematic toxic symptoms caused by infections of virus and bacteria and local and systematic lesions caused by endotoxins and exotoxins, and exhibits an excellence rate of 90%.
EP1894569A2 Tetracycline derivatives for treating cancer The invention is directed to the use of the compounds 9-amino- and 9-nitro-6-deoxy-5-hydroxytetracycline and of salts of these compounds for the treatment of cancer, especially of prostate cancer, breast cancer, melanoma or myeloma.
WO2011113047A2 Compositions and methods for characterizing breast cancer The invention provides compositions and methods for characterizing breast cancer stem In particular, the invention provides for the identification of cells expressing Twist and CD44 that express little or virtually undetectable levels of CD24 (i.e. a Twist+/CD44+/CD24-/low cell sub-population). The presence of such cells in a breast cancer specimen identifies the breast cancer as having increased metastic potential. Such cancers are identified as requiring aggressive therapies. Accordingly, the invention provides biomarkers suitable for identifying, diagnosing, and monitoring treatment of a subject with breast cancer.
CN101057840B Application of Vam3 in preparing medicine for treating chronic obstructive disease of lung The invention discloses the novel use of Vam 3 (Amurensin H) with a general formula (I) in preparing medicament for preventing and/or treating chronic obstructive pulmonary disease.
WO2007071442A3 Inhibitors of ccr9 activity N-(benzenesulphonyl)-2,3-dihydro-1H-indols, wherein the indol is substituted by cyano, carboxy or alkylcarbonyloxy and their use as therapeutical agents.
US20100216743 Therapy-enhancing glucan This invention provides a method for introducing substances into cells comprising contacting a composition comprising orally administered beta-glucan with said cells. This invention also provides a method for introducing substances into a subject comprising administering to the subject an effective amount of the above compositions. The substance which could be delivered orally includes but is not limited to peptides, proteins, RNAs, DNAs, chemotherapeutic agents, biologically active agents, plasmids, and other small molecules and compounds. Finally, this invention provides a composition comprising orally administered beta-glucan capable of enhancing efficacy of IgM and different uses of the said composition.
EP1569655A1 Use of selective progesterone receptor modulators for the treatment of androgen deficiency Methods of increasing testosterone levels using selective progesterone receptor modulators (SPRMs) are provided. SPRMs may therefore be used to treat conditions associated with decreased levels of testosterone such as sexual dysfunction, hypogondism, andropause, muscle wasting, and frailty. Compositions comprising SPRMs are also provided.
US20060122147 Combination preparation of hyaluronic acid and at least oe local anesthetic and the use thereof The invention relates to a combination preparation comprising an active agent A from the group hyaluronic acid, the salts and fragments thereof, at least one active agent B from the group of local anaesthetics and derivatives thereof and also if necessary further additives. These combination preparations are used for the medical treatment of degenerative and traumatic diseases of all joints, for the treatment of articular cartilage and cartilage bone defects and also meniscus and intervertebral disc lesions, such as e.g. arthrosis, articular rheumatism, osteochondritis dissecans, flake fractures, meniscus lesions and for the treatment of skin and mucous membrane changes, also from cosmetic aspects.
US7476693 Suramin and derivatives thereof as topical microbicide and contraceptive The present invention is directed to methods of inhibiting STDs by topically administering suramin or a derivative thereof to actual or potential sites of infection, and methods of preventing pregnancy by topically applying suramin or a derivative thereof intravaginally. Suramin compositions that include an antimicrobial agent and/or a sperm-function inhibitor are also provided and may advantageously be used in the methods of the invention. A method of simultaneously inhibiting STDs and preventing pregnancy is also provided. Devices impregnated or coated with the topical suramin compositions are further disclosed and may be used to apply the compositions described herein.
CN103405490A Compound medicine for preventing and treating infectious diseases of livestock and poultry and preparation method thereof The invention discloses a compound medicine for preventing and treating infectious diseases of livestock and poultry. The compound medicine comprises the following raw material medicine components in parts by weight: 25-35 parts of gynostemma pentaphylla, 30-40 parts of honeysuckle, 8-13 parts of taurine, 5-10 parts of kanamycin sulfate, 2-6 parts of fructo-oligosaccharide and 10-25 parts of auxiliary materials. The compound medicine disclosed by the invention has the synergistic effects of treating both symptoms and root causes for inflammations of livestock and poultry, reducing the probability on drug resistance of pathogenic bacteria, and enhancing the curative effect, improves the sensitivity and antibacterial effect and reduces the pharmaceutical failure caused by diagnostic reasons. The rate of survival of livestock and poultry is raised from original 90% to over 95%, and the morbidity is reduced from original 78.33% to below 6%. The protection rate of vaccine (titer) is increased. The composition is safe and non-toxic, and the utilization ratio of feed is increased. The compound medicine is convenient to use and simple in process of preparation method, and has stronger market competitiveness and better economic and social benefits.
CN103356633A Use of Aspeverin in preparation of drug for resisting helicobacter pylori (Hp) The invention discloses a use of Aspeverin in preparation of a drug for resisting helicobacter pylori (Hp). An in-vitro activity experiment shows that Aspeverin has strong Hp resistance activity. Aspeverin can be used for treatment on acute and chronic gastricism, gastric ulcer and duodenum ulcer and can be used for preparation of drugs for treating acute and chronic gastricism, gastric ulcer and duodenum ulcer. The use of Aspeverin in preparation of a drug for resisting Hp is disclosed in the invention for the first time. The Aspeverin has a novel type of a skeleton, has very strong activity of inhibiting Hp, does not get any revelation from other compounds, has obvious substantive features and obviously develops prevention and treatment on Hp infection.
CN102085182B Sinomenine hydrochloride slow-release injection and preparation method thereof The invention discloses a sinomenine hydrochloride slow-release injection and a preparation method thereof. The slow-release injection comprises one of a synthetic high molecular polymer nanoparticle sinomenine hydrochloride slow-release injection, a natural high molecular material microsphere sinomenine hydrochloride slow-release injection, a liposome sinomenine hydrochloride slow-release injection, a multi-vesicle liposome sinomenine hydrochloride slow-release injection and a gel sinomenine hydrochloride slow-release injection. In the invention, various sinomenine hydrochloride slow-releaseinjections prepared by different methods can prolong drug action time, reduce medication frequencies, maintain relatively stable in-vivo blood concentration and reduce toxic side effects of drugs.
US6989382 Enzyme inhibitors; pyridin-2-yl-amino-ethyl-amino-phenyl derivatives; diabetes, Alzheimer's disease, Parkinson's disease, Huntington's disease, obesity, cardiovascular disease, hypertension, polycystic ovary syndrome, ischemia, brain injury New carbocyclic compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease, other neurodegenerative disorders, such as Parkinson's disease and Huntington's disease, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
CN103110869A Extraction method of strong loquat syrup The invention provides an extraction method of a strong loquat syrup. Except for menthol and pericarpium papaveris, all the other 5 medicinal materials in the formula are decocted in water for two or three times; the decoctions are filtered, the filtrates are blended with each other and then concentrated; and then the concentrate is added with auxiliary materials; besides, the pericarpium papaveris is decocted in acid water for 2 hours twice. The process provided by the invention improves the extraction transfer rate of the alkaloid in the raw materials of the strong loquat syrup; the transfer rate of the alkaloid is increased to about 30% from 10% in the past; and therefore, the clinical curative efficacy is greatly improved.
CN101024086A Composition formed from chitosan and its derivatives and low-molecular heparin and pneparation and preparing method The present invention belongs to the field of medicine technology. In particular, it relates to a compound made up by using chitosan, its derivative and low-molecular heparin, its preparation and preparation method. Said compound can raise stability of low-molecular heparin, and can further raise bioavailability of said medicine preparation. Said compound can be made into various oral preparations, injection, spray, nose drops, aerosol and suppository, etc.
CN1931139A Freeze dried ligustrazine hydrochloride prepn for injection and its prepn process The present invention is freeze dried ligustrazine hydrochloride preparation for injection and its preparation process, and features that the freeze dried ligustrazine hydrochloride preparation contains the main medicine material ligustrazine hydrochloride in 5-100 wt% and supplementary material of at least one of mannitol, sorbitol and dextran in 0-95 wt%. The preparation process includes the following steps: 1. adding the main and supplementary material as well as water for injection into some container, heating to 35-40 deg.c and stirring for dissolving; and 2. adding active carbon into the solution, stirring, filtering, straining with microporous filtering membrane, measuring ligustrazine hydrochloride content, packing, etc. The freeze dried ligustrazine hydrochloride preparation for injection has long effective period over three years.
US20090306117 Rosuvastatin zinc salt The present invention is related to rosuvastatin zinc salt of the Formula (I), process for preparation thereof and medicinal products containing said salt. Rosuvastatin zinc salt according to the present invention is prepared by reacting rosuvastatin with a zinc alcoholate, zinc enolate or an inorganic or organic zinc salt and isolating the thus obtained rosuvastatin zinc salt (2:1).
US20120302619 Novel 1-aryl-3-Azabicyclo[3.1.0]Hexanes: Preparation And Use To Treat Neuropsychiatric Disorders The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.
CA2670211A1 Teeth bleaching compositions and devices The present invention is directed to an oral care device configured to contact teeth, where the device includes disposed therein a bioactive glass in an amount effective to mineralize teeth when contacted with the teeth under conditions effective to mineralize the teeth; and a tooth-bleaching agent in an amount effective to whiten teeth when contacted with the teeth under conditions effective to whiten the teeth, and to methods for simultaneously mineralizing and whitening teeth utilizing the devices of the present invention.
EP2671582A1 Ring-fused heterocyclic derivative A ring-fused heterocyclic derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof having a T-type calcium channel regulatory effect and useful as a pruritus therapeutic and/or preventive agent, and the like are provided. In the general formula (I), R1 represents optionally substituted lower alkyl, and the like; R2 represents an optionally substituted cycloalkyl, and the like; Q represents a hydrogen atom, and the like; R3 represents -C(=O)NR8R9 (wherein R8 and R9 may be the same or different, and each represents a hydrogen atom, and the like), and the like; L1 represents -CR11AR11B- (wherein R11A and R11B may be the same or different, and each represents a hydrogen atom, and the like), and the like; and W1 and W2 may be the same or different, and each represents C-R12 (wherein R12 represents a hydrogen atom, and the like), and the like.
CN1559404A Method for preparing artemisine and its liposoluble derivatives emulsion An emulsion of artemisine and it sliposoluble derivative for treating lung cancer, liver cancer, lymph cancerand arrhythmia is prepared through proportionally mixing lecithin or soybean phosphatide, ginghaosu or its liposoluble derivative, and surfactant,and emulsifying in ultrasonic hydrated oil for injection.
US7151092 Cytarabine monophosphate prodrugs Compounds of Formula I, their preparation and uses are described: wherein: M and V are cis to one another and MH is cytarabine; the 5′ oxygen of said cytarabine is attached to the phosphorus; V is 4-pyridyl; and pharmaceutically acceptable prodrugs and salts thereof.
WO2006073572A2 Treatment of conditions caused by calcium abnormalities In certain aspects, the invention relates to use of PKD2 agonists, such as triptolide and triptolide derivatives, to regulate calcium release. In other aspects, the invention relates to use of PKD2 agonists to treat or aid in the treatment of any condition in which a calcium channel, such as the gene product of PKD 1 and/or PKD2, is mutated; calcium signaling is abnormal; or both, such as polycystic kidney disease.
CN101849905A Voriconazole eye drops and preparation method thereof The invention discloses voriconazole eye drops. Every 1000 milliliters of eye drops contain 3-50g of voriconazole powder, 20-500g of hydroxypropyl-beta-cyclodextrin, 0.1-0.3g of bacteriostat, 0.5-2.5g of sodium hyaluronate and the balance of water for injection, wherein the bacteriostat is benzalkonium chloride, benzalkonium bromine or ethylparaben. The invention also discloses a preparation method of the voriconazole eye drops. The invention greatly increases the solubility of voriconazole in water to 0.3-5%, so that the medicine can exist in water solution in the form of molecules, thereby providing convenience for exerting the antifungal action of the medicine. Meanwhile, when being applied to eyes, the invention provides convenience for exerting the antifungal action of the medicine through cornea. The preparation method can be carried out at room temperature without affecting the medicine stability, and has the advantages of simple and easy realization and low cost.
WO2006053766A1 Methods for purifying trans-(-)-δ9-tetrahydrocannabinol and trans-(+)-δ9-tetrahydrocannabinol Methods for making trans-(-)-Δ9-tetrahydrocannabinoI and trans-(+)-Δ9-tetrahydrocannabinol are disclosed herein. In one embodiment, a trans-(-)-Δ9-tetrahydrocannabinoI composition is prepared by allowing a composition comprising (±)-Δ9-tetrahydrocannabinol to separate on a chiral stationary phase to provide a trans-(-)-Δ9-tetrahydrocannabinoI composition comprising at least about 99% by weight of trans-(-)-Δ9-tetrahydrocannabinol based on the total amount of trans-(-)-Δ9-tetrahydrocannabinol and trans-(+)-Δ9-tetrahydrocannabinol. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of a trans-(-)-Δ9-tetrahydrocannabinoI having a purity of at least about 98% based on the total weight of cannabinoids.
WO2010095428A1 Foxm1 peptides and vaccines containing the same The present invention provides isolated peptides having the amino acid sequence of SEQ ID NO: 34 or fragments thereof, which bind to HLA antigen and induce cytotoxic T lymphocyte (CTL). The present invention further provides peptides which include one, two, or several amino acid insertions, substitution or addition to the aforementioned peptides or fragments, but still have the cytotoxic T cell inducibility. Further provided are nucleic acids encoding any of these aforementioned peptides as well as pharmaceutical substances or compositions including any of the aforementioned peptides or nucleic acids. The peptides, nucleic acids, pharmaceutical substances or compositions of the present invention may be used for treating cancer or tumor.
US20080004318 Substituted Bicyclic and Tricyclic Thrombin Receptor Antagonists Substituted bicyclic and tricyclic modified himbacine derivative of the formula: or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.
CN102442918A Stable levocarnitine compound The invention specifically relates to a levocarnitine sesquihydrate, which belongs to the technical field of medicines. The levocarnitine sesquihydrate obtained in the invention contains one and a half crystal water and has the advantages of a high purity and good stability, having non-obvious moisture absorption and weight gain even under the condition of high humidity. The invention also relates to application of the levocarnitine sesquihydrate in preventing and mitigating myocardial damage, in mitigating and alleviating symptoms of chest pain, in treating coronary heart disease, angina pectoris, heart failure, myocardial infarction and cerebral infarction, in auxiliary treatment of renal disease, chronic pulmonary heart disease, male sterility, acquired immune deficiency syndrome, intermittent claudication, as well as acute and chronic hepatitis, cirrhosis, chronic hepatic insufficiency, muscular atrophy, diabetes and bad postpartum uterus contraction, etc.
CN101972251A Use of hirsutine in preparing anti-addictive drug The invention relates to a drug containing a heterocyclic system of a hexatomic ring with nitrogen as a heteroatom, in particular to an application of hirsutine in preparing a drug for preventing and treating opioid substance addiction or amphetamine substance dependence. The drug is composed of the hirsutine and a pharmaceutically acceptable auxiliary material, wherein, the hirsutine content is 5-85%. The drug is oral preparation such as a tablet or a capsule and the like.
CN103610677A Repaglinide troche and preparation method thereof The invention relates to an oral troche which contains repaglinide or pharmaceutically acceptable derivatives of repaglinide as well as a preparation method of the oral troche. According to the preparation method, powder of repaglinide or pharmaceutically acceptable derivatives of repaglinide is directly pressed into troche, so that the production cost is remarkably lowered, and the disintegration and the dissolution rate are greatly improved. The bioavailability and the stability of the medicine can be improved, and the problem of low content uniformity of existing small-dose medicines formed by the direct pressing method is overcome, so that the quality of the troche is better guaranteed.
WO2014121633A1 Derivative of homoserine lactone, and preparation method and use thereof Disclosed are a derivative of homoserine lactone shown in formula I, and a preparation method and use thereof. The compound has a function of sensing and regulating a bacterial colony, and can be used for prevention and/or treatment of related diseases caused by bacterial infection.
US20090175801 Cns-tumor treatment method and composition A method, aerosol composition, and aerosolizing device for treating a brain tumor in a subject are disclosed. The method includes intranasally administering to the subject, an amount of a telomerase inhibitor, such as an oligonucleotide telomerase inhibitor, effective to inhibit growth of the tumor in the subject.
US20050027007 Allylamides useful in the treatment of alzheimer's disease Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula (I) where R1, R2, R3, B, J1, J2, X and Z are as defined herein.
CN103622961A Application of non-peptide bradykinin B2 receptor stimulant in prompting hair growth The invention belongs to the technical field of medicaments, and relates to a novel application of a non-peptide bradykinin B2 receptor stimulant in prompting hair growth in partial application. The invention innovatively discovers that the non-peptide bradykinin B2 receptor stimulant has a good hair growth prompting function, and research shows that the action mechanism of the stimulant in prompting hair growth is that the non-peptide bradykinin B2 receptor stimulant is capable of stimulating a bradykinin B2 receptor to cause release of endogenous prostaglandin F-2a or prostaglandin E, and partial microenvironment is improved through receptor way of the prostaglandin so as to prompt hair growth, and therefore the effect of prompting hair growth is achieved. The invention provides a new way for research and development of new target spot medicaments for treating various hair loss diseases.
CN102548987A Fluoro-substituted compounds as kinase inhibitors and methods of use thereof The present invention provides for novel compounds of Formula I and pharmaceutically acceptable salts and solvates thereof which have kinase inhibitor activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating and preventing a Bcr-Abl, c-Kit or PDGF-R mediated disorder for which one or more kinase inhibitor is indicated, including neoplasia such as chronic myelogenous leukemia or gastrointestinal stromal tumors. The present invention also provides for processes of making the compounds of Formula I, including salts and solvates thereof, and pharmaceutical compositions comprising the same.
US20050187302 administering the selective estrogen receptor modulator ospemifene, 2-(4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy)ethanol This invention relates to a method for the treatment or prevention of osteoporosis in an individual suffering from increased bone turnover, said method comprising administering to said individual an effective amount of a therapeutically active compound, which is a selective estrogen receptor modulator of the triphenylalkene or triphenylalkane structure.
US20090281149 Amine Derivative Compounds for Treating Ophthalmic Diseases and Disorders Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
CN101933921B Composition of Doripenem and amino acid The invention relates to a composition containing Doripenem, in particular to a composition containing the Doripenem and amino acid, wherein the amino acid is selected from one ore some of aminopropionic acid, phenylalanine, aminocaproic acid and threonine.
WO2011108930A1 A MiRNA MOLECULE DEFINED BY ITS SOURCE AND ITS DIAGNOSTIC AND THERAPEUTIC USES IN DISEASES OR CONDITIONS ASSOCIATED WITH EMT The invention relates to the diagnostic and therapeutic uses of a miRNA molecule or an equivalent thereof wherein a source of said miRNA molecule or equivalent thereof comprises at least 80 nucleotides and comprises a motif having at least 98% identity with the motif represented by SEQ ID NO:1 or a source thereof in a disease and condition associated with EMT (Epithelial to Mesenchymal Transition).
CN103239450A Rapidly-dissolving and stabile montelukast oral solid preparation and preparation method thereof The invention relates to a rapidly-dissolving and stabile montelukast oral solid preparation and a preparation method thereof, wherein the preparation uses montelukast as a raw material drug, is added with a diluents, a disintegrating agent, an additive, an adhesive and a lubricant as auxiliary materials, and uses a pharmaceutically acceptable preparation technology. The preparation and the preparation technology can raises a dissolving speed of the oral preparation, enables the oral preparation to substantially raise the dissolving speed in a dissolving mediums of pH1.0 and pH 4.5, and can raises the medicament stability.
CN101367816A Carbpenem derivants The present invention belongs to the technical field of medicine, in particular to a carbapenem derivative shown in the formula (I) and a pharmaceutically acceptable salt, an easily hydrolyzed ester, an isomer, a hydrate and a hydrate of the ester or the salt thereof: wherein, R<1>, R<2>, R<3>, R<4> and R<5> are defined in the description. The present invention also relates to preparation methods of the compounds, drug combinations and applications of the compounds in the preparation of drugs for treating and/or preventing infective diseases.
US7384937 Antiarthritic agents; multiple sclerosis ; organ rejection ; antidiabetic agents; inflammatory bowel disorders; antiischemic agents; skin disorders Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein, and analogs thereof are provided which are useful in treating leukocyte activation-associated disorders.
EP2185570A2 Novel activators of glucokinase The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistence and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
CN102935064A Aspartic acid lomefloxacin injection preparation and preparation method thereof The invention belongs to the field of chemicals and particularly relates to an aspartic acid lomefloxacin injection preparation and a preparation method thereof. Aspartic acid lomefloxacin, a cosolvent and a stabilizer are subjected to processes of liquid matching, encapsulation, nitrogenization, sterilization, light inspection, complete inspection and the like to form an injection, the injection is stored for three months at the temperature of 2 DEG C to 8 DEG C under the condition of low temperature refrigeration, and the separation by crystallization is absent. According to the aspartic acid lomefloxacin injection preparation and the preparation method thereof, quality guarantee is provided for medication safety of patients.
US7498360 Adminisering prostaglandin into ear A novel method and compositions for the local treatment of Meniere's disease, tinnitus and hearing loss are described. The treatment is based on the administration of a therapeutically effective amount of a prostaglandin of the F-type to the inner ear. The treatment can be either continuous or intermittent and may involve the use of pumps, gels, or slow release drug inserts.
US20120136031 P38map kinase inhibitor The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers and tautomers, which is an inhibitor of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
EP1734953A1 Co-formulations of kits of bioactive agents Provided, among other things, is a formulation or kit comprising: (a) a pharmaceutically effective dosage of one or more a glucose-level-controlling bioactive agents selected from an α-glucodase inhibitor, sulfonylurea, meglitinide, thiazolidinediones, biguanide, insulin, dual PPAR α/Ϝ agonist, PPARy agonist or insulin secretagogue; and (b) a pharmaceutically effective dosage of (i) one or more of an antihypertensive bioactive agent selected from an ACE inhibitor, calcium channel blocker, beta blocker, angiotension II receptor antagonist or diuretic, or (ii) one or more of an anti-dyslipidemia bioactive agent selected from a HMG-CoA reductase inhibitor, bile acid sequestrant, fabric acid derivative, sterol, cholesterol absorption inhibitor, MTP inhibitor or nicotinic acid derivative; wherein: in the case of (i) a combination of a first bioactive agent of group (a) that is metformin with a second bioactive agent of group (b), or (ii) a combination of a first bioactive agent of group (a) that is a thiazolidinedione or dual PPAR α /Ϝ agonist with an angiotension II receptor antagonist, one or more of the following applies: (I) one of the first bioactive agent or the second bioactive agent is formulated for sustained release, and the other is formulated for immediate release, each formulated for once-a-day dosing; or (II) the co-formulation or kit comprises (A) a biguanide and a thiazolidinedione and (B) one or more group (b) bioactive agents.
WO2014017787A1 Pharmaceutical composition having antidiabetic and antiobesity activities The present invention provides a pharmaceutical composition for preventing and treating diabetes, or a pharmaceutical composition for preventing and treating obesity. The pharmaceutical composition for preventing and treating diabetes according to the present invention has the effect of significantly reducing blood sugar, and also exhibits antidiabetic effects that are almost equal to those of metfornin which has been mostly used as a therapeutic agent for type 2 diabetes. The pharmaceutical composition for preventing and treating obesity according to the present invention significantly reduces the weight and size of fatty cells in an experimental animal which was fed with a high fat diet, and also exhibits the effects of reducing weight and fat which are equal or superior to those of orlistat which has been used as a therapeutic agent for obesity.
US20120252874 Methods for delivery of sirna to the spinal cord and therapies arising therefrom The present application relates at least in part to methods for the administration of small interfering RNAs (siRNAs) to the spinal cord of a human or animal patient and also to a method of treatment for spinal cord injury and other diseases and disorders of the CNS. In particular, the application discloses methods to deliver an siRNA compound locally, directly and without the need for transduction vehicles and formulations in effective doses to the injured spinal cord to promote recovery of CNS function and or attenuation of allodynia.
CN101229175A Medical applications of couple protopanoxadiol derivatives and compound body thereof The invention belongs to a medicine technical field, relating to a medical usage of a couple of Protopanaxadiol derivatives and the compound thereof. The coupled compound is named 20(R)-25-hydroxy-Dammarane-3 Beta, 12 Beta, 20-triol and 20(S)-25-hydroxy-Dammarane -3 Beta, 12 Beta, 20-triol [20(R)-25-hydroxyl-dammarane-3 Beta, 12 Beta, 20-triol (abbreviated as 25Rhdt) and 20(S)-25-hydroxyl-dammarane-3 Beta, 12 Beta, 20-triol (abbreviated as 25Shdt)]. The 25Rhdt and the 25Shdt and the compound thereof have the anti-tumor activity for controlling the growth and proliferation of the human tumor cells, inducing the differentiation and death of the tumor cells, controlling the creation of the rebirth blood tube of the tumor, controlling the moist and transfer of the tumor, improving the human immunity and reducing the side effect of the chemotherapeutic drugs. The 25Rhdt and the 25Shdt and the compound thereof can be made into any medical formulation for treating different cancers and are mainly applied to the prevention and cure of all kinds of the above-mentioned malignant tumors with the important exploitation value and application outlook.
EP2493296A1 Alleviating oxidative stress disorders with pufa derivatives Some aspects of the invention provide for essential fatty acids which are substituted in specific positions to slow down oxidative damage by Reactive Oxygen Species (ROS), and to suppress the rate of consequent formation of reactive products, for the purpose of preventing or reducing the damage associated with oxidative stress associated diseases such as neurological diseases and age-related macular degeneration (AMD).
CN102451155A Prescription and preparation method of docetaxel injection The invention provides a prescription and a preparation method of an anti-tumor medicament docetaxel injection which is used for early chemotherapy failure or metastatic breast cancer, late cisplatin chemotherapy failure or metastatic small cell carcinoma in the field of pharmacy. The preparation is an injection prepared by using docetaxel as an active component and adding injection auxiliary materials through heat source removing, degerming and alcohol volatilization. Aiming at the overcoming the defect of a medicinal preparation using docetaxel as the active component, the invention provides the prescription and preparation method of the docetaxel injection. The preparation prepared by virtue of the method is excellent in stability and convenient in preparation, so that the medicament safety and the patient adaptability are improved.
CN101314044B Oxidation resistance ligand functionalized golden nano-complexes, preparation method and application thereof The invention discloses a gold nano composition with oxidation resisting aglycone function, a preparation method thereof and an application thereof. In the gold nano composition with oxidation resisting aglycone function, surfaces of gold nano particles are connected with oxidation resisting aglycones with formula I structure by connexons with formula II structure, the oxidation resisting aglycones are connected with R radical ends of the connexons, the gold nano particles are connected with sulfhydryl ends of the connexons, and in formula II, R is NH or O, and n is an integer from 2 to 11. The tests conducted by the investor of the invention determine that the gold nano composition with oxidation resisting aglycone function has quite high oxidation resisting activity and can be widely used as a highly efficient antioxidant.
CN101703559B Medicinal composition with function of relieving visual fatigue and preparation method thereof The invention discloses a medicinal composition with a function of relieving visual fatigue and a preparation method thereof. The medicinal composition is prepared from cowberry extract, lutein and vitamin A in certain weight ratio. The medicinal composition can be prepared into tablets, capsules, granules, pills, powder, oral administration liquid preparations, wherein the preferable dosage formis soft capsule.
WO2010066852A1 Composition comprising isoflavones A composition comprising at least one isoflavone, phloridzin and one or more probiotics. A composition as described herein is also provided for internal use as a natural alternative to hormone replacement therapy and for treating disorders such as menopause and correlated symptoms, alcoholism, stress, insomnia, obesity and cellulite.
CN103374013A Salt of dihydrosanguinarine derivative The invention relates to fumarate or pharmacological acceptable solvates of dihydrosanguinarine and derivatives of the dihydrosanguinarine as well as an application of the fumarate or pharmacological acceptable solvates to the preparation of drugs for treating hepatitis B.
US20100240713 Aromatic and heteroaromatic compounds useful in treating iron disorders This invention is directed to compounds of formula (I), wherein m, formula (II), R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.
CN101143173A Capsule for treating acute dysentery and acute diarrhea and its preparation method The invention provides a capsule dosage for remedying the acute dysentery and the acute diarrhea and the preparation method of the capsule dosage. The raw materials are a berberine hydrochloride, a common aucklandia root and a prepared medicinal evodia fruit. The preparation method is that firstly partial common aucklandia root is crushed as fine powder; then the residual common aucklandia root is crushed as coarse powder to be mixed with the prepared medicinal evodia fruit, and volatile oil is collected by the method of water distillation and is embedded by beta-cyclic dextrin; the liquid medicine after distillation is filtered, and the filtrate is collected, and the medical residue is boiled for 0.5 to 2 hours in water to be filtered; the filtrate of the two times are combined to be concentrated by reducing pressure and be dried by spray to form dry extract powder; the berberine hydrochloride and the fine powder of the common aucklandia root are mixed with the dry extract powder to be pelletized and dried and is added with the embedded content of the beta-cyclic dextrin to be encapsulated to form the capsule dosage. The drug of the invention has quite significant action of promptly eliminating the symptoms of the abdominal flatulence, the bellyache, the abdominal fullness etc. Because the dosage type of capsule is adopted with loose medical materials structure, the capsule dosage can be disintegrated inside the gastrointestinal tract at a quite high speed, and the pharmacological function can act in time.
US20080090850 Herpetic neuralgia topical treatment Compositions and methods for treatment of acute herpetic zoster and post herpetic neuralgia. The compositions comprise the combination of five or six components, namely, a carrier penetrator, an anti-inflammatory agent, a topical analgesic, a nonsteroidal anti-inflammatory penetrator, a direct-application anti-viral agent, and, optionally, an anti-convulsant and calcium-channel blocker. The compositions are formulated to be applied topically to the affected areas.
CN1732975A Prescription of compound electrolyte drug for injection and method for preparing the same Disclosed is a prescription of compound electrolyte drug for injection, which comprises sodium chloride 175 parts, potassium chloride 150 parts, and sodium lactate 224 parts. The dosage types include powder injection or small volume injection.
US20080064645 A carbohydrate linked to a fluorophore through a 2-amido-2-(1-hydroxyalkyl)ethoxy linkage; inhibition of caveolar endocytosis, plasma membrane microdomain formation, virus binding and infection, transmembrane signaling, and integrin function in cells; anticarcinogenic and antiinflammatory agents This disclosure provides a composition useful for inhibiting caveolar endocytosis, plasma membrane microdomain formation, virus binding and infection, transmembrane signaling, and integrin function in cells. The composition is composed of non-natural analogs of sphingolipids, and may have applications in the treatment or amelioration of diseases associated with caveolar endocytosis, plasma membrane microdomain formation, transmembrane signaling, and integrin function. Methods for making and using the described composition are also provided.
US8557852 Methods of using crystalline forms of a salt of a factor Xa inhibitor The present invention provides methods for preventing or treating a condition characterized by undesired thrombosis in a mammal using a crystalline polymorph form of a maleate salt of a compound of Formula I that has activity against mammalian factor Xa.
US20100222343 Phosphoinositide 3-kinase inhibitors with a zinc binding moiety The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
WO2013090722A1 Trpc4 modulators for use in the treatment or prevention of pain The instant application discloses methods of treating, reducing, or preventing pain in a mammal, which may include administering a compound capable of modulating a transient receptor potential channel. In one aspect, the TRP channel may be TRPC4. Types of pain contemplated by the present disclosure include acute, chronic, neuropathic, and nociceptive pain.
US20080161406 Novel formulations of alpha-2,4-disulfophenyl-N-tert-butylnitrone Novel pharmaceutical formulations of α-(2,4-disulfophenyl)-N-tert-butylnitrone and pharmaceutically acceptable salts thereof and the use of such formulations in the treatment of various diseases and conditions, especially stroke, are disclosed.
US20080064745 Androgen Modulators The present invention is directed to the compound 4-(2-methoxy-phenoxy)-2-trifluoromethyl-benzonitrile, is use as an androgen modulator and to pharmaceutical compositions containing this compound.
US20120016027 Composition and Method for Improved Lens Comfort The present invention relates to methods of preventing ocular discomfort, improving ocular comfort or ameliorating decrease in ocular comfort during wearing of an ophthalmic device (such as a contact lens), that include the administration of compositions comprising fatty acids, such as omega-3 and/or -6 fatty acids. The present invention also relates to fatty acid compositions suitable for use in the methods of the present invention.
WO2005115367A3 Modulation of neurotransmitter activity in neurons The present invention relates generally to methods, devices and compositions for treating mental, neurological, and cognitive diseases related to deficiencies in the biosynthesis and/or metabolism of neurotransmitters, wherein the neurotransmitter is acetylcholine, nitric oxide, histamine, norepinephrine, a bioactive amine, an amino acid or a neuropeptide, veratridine, curare, tetrodotoxin, f lunarizine, calσicludine, and omega -cono toxin; wherein the bioactive amine is selected from the group consisting of dopamine, epinephrine, norepinephrine, serotonin; wherein the amino acid is selected from the group consisting of glutamate, glycine and gamma- aminobutyric acid (GABA) ; the neuropeptide is selected from the group consisting of enkephalins, dynorphins and substance P and the psychological disorder is selected from the group consisting of addiction, substance abuse, autism, dyslexia, obsessive- compulsive disorder, generalized anxiety disorder, post- traumatic stress disorder, panic attacks, social phobia, major depression, bipolar disorder and schizophrenia, tardive dyskinesia, Huntington's disease, and Parkinson's disease.
CN101756999A Medicine composite for treating trichomadesis The invention discloses a medicine composite for treating trichomadesis, aiming to provide a medicine composite which can stimulate scalp tissues and hair follicles through hypodermic infection to regenerate hairs so as to cure trichomadesis. The medicine composite is prepared by mixing selected raw material medicines of triamcinolone acetonide, dolicaine, vitamin 12 injections and Atropine injections in weight percentage of 10:10:10:1; and the drug composite can be injected on an affected part subcutaneously. The medicine composite is easy to prepare, is convenient to use and can direct act on the affected part to regenerate hairs by stimulating the scalp tissues and the hair follicles, therefore, the invention has the advantages of fast curative effect, non relapse and easy treatment.
CN103044523A Dexamethasone-RGD polypeptide conjugate, preparation method thereof and application The invention relates to a dexamethasone-RGD polypeptide conjugate shown as general formula i, a preparation method thereof and application. In the formula i, RGDX is tetrapeptide Arg-Gly-Asp-X, wherein X is any amino acid of Val, Phe and Ser. Proved by experiments, the compound of the present invention has excellent immunosuppressive effect and anti-inflammatory effect, and the side effects of osteoporosis is reduced. The conjugate can be used as an immunosuppressant and anti-inflammatory agent for the side effect of low osteoporosis clinically. At the same time, the dexamethasone-RGD polypeptide conjugate of the present invention can self-assemble into stable nanoparticles with particle size of 200-500 nm, therefore the conjugate can be prepared into a target drug of immunosuppressive pharmacosome, microemulsion or liposome.
WO2005040172A1 Tricyclic proline derivative A novel tricyclic proline derivative which has antitumor activity and is effective in inhibiting skin aging, improving skin nature, or remedying wounds, dermatitis, or arthritis. It is a compound represented by the formula (I): (I) (wherein R1 represents hydroxy, lower alkoxy, lower alkynyloxy, lower alkylsulfanyl, (un)substituted arylalkyloxy, (un)substituted heteroarylalkylsulfanyl, cycloalkylmethoxy, etc.; and R2 represents (un)substituted aryl, (un)substituted heteroaryl, etc.) or a pharmaceutically acceptable salt or another derivative of the compound.
CN101889989A Amoxicillin enteric controlled-release preparation composite and preparation method thereof The invention discloses an amoxicillin enteric controlled-release preparation composite and a preparation method thereof. The composite is mainly prepared from amoxicillin bulk substance, slow-releasing material, enteric material and proper accessories. By using the amoxicillin enteric controlled-release preparation provided by the invention, amoxicillin can not disintegrate in the stomach and not stimulate the gastric mucosa, thus avoiding adverse reactions such as decreased appetite, nausea, bellyache and diarrhea which are caused by taking the medicine; and the release rate of the medicine can be reduced, the frequency of use can also be reduced and the patient compliance can be improved. The invention provides a new preparation with higher safety and better patient compliance, and the quality controllability and stability of the preparation technology are good.
US20110003870 Method of treatment of a neurological disorder A method of treating neurological conditions, such as Parkinson's Disease and Restless Leg Syndrome, in a mammalian subject is disclosed. The method comprises the administration of a once-a-day controlled release formulation of pramipexole, which formulation provides a consistently ascending PK profile during sleeping hours.
WO2005030734A1 Diaminopyrimidine derivatives as selective growth hormone secrectgogue receptor (ghs-r) antagonists The present invention is related to compounds of formula (I), (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, obesity and disorders associated with obesity such as non-insulin dependent diabetes mellitus.
US20100093810 Pharmaceutical Compositions for Reducing Amyloid Deposition, Amyloid Neurotoxicity, and Microgliosis The present invention provides methods for reducing Aβ deposition, Aβ neurotoxicity and microgliosis in an animal or human afflicted with a cerebral amyloidogenic disease, such as Alzheimer's disease (AD), by administering therapeutically effective amounts of the (R)-enantiomer of the dihydropyridine compound nilvadipine, also known as (−)-nilvadipine, to the animal or human, or by administering a non-racemic enantiomeric mixture of the dihydropyridine compound nilvadipine, to the animal or human. Further provided are methods for reducing the risk of Aβ deposition, Aβ neurotoxicity and microgliosis in animals or humans suffering from traumatic brain injury by administering (−)-nilvadipine, or non-racemic mixture of nilvadipine enantiomers, after the traumatic brain injury and continuing treatment for a prescribed period of time thereafter.
CN1859905A Method of controlling particle size of retinoic acid nanoparticles coated with polyvalent metal inorganic salt and nano particles obtained by the controlling method It is intended to provide a method of controlling the particle size of retinoic acid nanoparticles having relieved irritation, which can be subcutaneously and intravenously administered, is usable as a sustained release preparation, and has such a high skin-permeability as allowing the use thereof as an external preparation such as a drug or a quasi drug as well as a cosmetic to be applied to the skin, etc., and nanoparticles obtained by the controlling method. More specifically speaking, the controlling method comprises dispersing a solution of retinoic acid in a lower alcohol together with an aqueous alkali solution, further adding a nonionic surfactant thereto to give a mixture micell, adding a metal chloride or acetate and an alkali metal carbonate or phosphate at a molar ratio of from 1:0 to 1.0 to thereby form a film of a polyvalent metal inorganic salt on the micell surface, and then regulating the particle size to 5 to 300 nm. As the polyvalent metal inorganic salt, use is made of calcium carbonate, zinc carbonate or calcium phosphate.
US20090298813 Use of neuroprotective compounds in obtaining medicaments intended for the treatment of neurodegenerating diseases Use of neuroprotective compounds in obtaining medicaments intended for the curative treatment of neurodegenerative disease and/or the prevention of the appearance of disorders ensuing from those diseases.
US20080279867 Prevent trabsplant rejection; autoimmune diseases The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
CN103610696A Water-soluble calculus bovis factitius composition as well as preparation method and application thereof The invention relates to a water-soluble calculus bovis factitius composition as well as a preparation method thereof. The water-soluble calculus bovis factitius composition is mainly prepared from the following raw materials: calculus bovis factitius basic remedy mixture, solid polyethylene glycol, cyclodextrin and water-soluble auxiliary materials, wherein the calculus bovis factitius basic remedy mixture can provide the efficacy of the calculus bovis factitius in the prior art, the solid polyethylene glycol and the calculus bovis factitius basic remedy mixture can form a stable dispersion to protect the stability of the efficacy, the cyclodextrin is used for including the dispersion to form an inclusion complex of the calculus bovis factitius basic remedy mixture, the water-soluble auxiliary materials are used for substituting the insoluble auxiliary material components in existing calculus bovis factitius, so that on the basis of maintaining the original efficiency of the calculus bovis factitius, not only can the taste of the water-soluble calculus bovis factitius composition be improved, but also the water solubility and stability of the water-soluble calculus bovis factitius composition can be greatly improved.
CN103341140A Chinese patent medicine used for promoting gastrointestinal function and preparation method thereof The invention discloses a Chinese patent medicine used for promoting gastrointestinal function. The Chinese patent medicine is prepared from the following raw materials in parts by weight: 18 to 30 parts of rhizoma dioscoreae, 8 to 10 parts of rock candy, 5 to 12 parts of cricket, 8 to 14 parts of cassia twig, 15 to 22 parts of radix paeoniae alba, 10 to 18 parts of rhizoma zingiberis, 10 to 18 parts of colla corii asini, 5 to 10 parts of roasted rhizoma atractylodis macrocephalae, 16 to 22 parts of platycodon grandiflorum, and 12 to 18 parts of mirabilite. The use result shows that the Chinese patent medicine has the advantages as follows: the curative effect is high, the effective rate in chronic gastritis treatment is up to more than 95%; the curative effect in chronic enteritis treatment and colitis treatment is remarkable, and the total effective rate is up to more than 85%; the cost is low, so that the economical burden of a patient is low, and the social and economic benefits are remarkable; and natural foot botanical medicines homologous in diet medication are adopted as the raw materials, all components meet the specifications of drug administration regulations and have neither noxious nor side effect upon a human body.
EP0783514B2 Sterol compositions from pulping soap A process for purifying and preparing phytosterol compositions from pulping soap comprises extracting from the pulping soap a creamy precipitate and purifying this precipitate to form the composition.
US20090258914 Inhibitor of Anti-Apoptotic Proteins A compound having the structure A is described as well as the use of such compounds to inhibit at least one BCL-2 protein family member.
CN102716107A Water-soluble ibuprofen pharmaceutical composition The invention discloses an ibuprofen pharmaceutical composition, comprising ibuprofen, arginine and tween. According to the invention, by adding tween in the ibuprofen and arginine solution, the stability of the ibuprofen pharmaceutical composition in clinic application is improved. Experiments show that the ibuprofen pharmaceutical composition solution can be stable for 48 hours after being diluted by using normal saline, glucose injection or Sodium Lactate Ringer's Injection.
US8420112 Solid dosage form for treating headaches A retrievable, sustained release, solid dosage form is provided for implanting into cranial bony canals and for prolonged release of an anesthetic, whereby treating neurovascular conditions, such as migraine. The dosage comprises an anesthetic contained in a polymeric carrier, and a retrieval member, the anesthetic being gradually released from the carrier.
CN101103993A Hypoglycemic medicine composition The invention relates to a newly-developed medicine compound for diabetes which contains sulfonylureas drug for diabetes or a bioactive metabolite of the sulfonylureas drug for diabetes or pharmaceutical salt of the sulfonylureas drug for diabetes, and thiazolidinedione drug for diabetes or pharmaceutical salt and vitamin B of the thiazolidinedione drug for diabetes. The compound contains the sulfonylureas drug for diabetes of therapy dose or the bioactive metabolite of the sulfonylureas drug for diabetes or the pharmaceutical salt of the sulfonylureas drug for diabetes, the thiazolidinedione drug for diabetes of therapy dose or the pharmaceutical salt and therapy dose of vitamin B of the thiazolidinedione drug for diabetes or compound which is related to the thiazolidinedione drug for diabetes and has similar bioactivity and pharmaceutical carrier or excipient. The invention also relates to the purpose of the compound in preparation of drug for treating diabetes or preventing diabetes complication, belonging to the pharmaceutical field.
US20070099876 Target directed chemotherapy of tumours of the sexual organs The invention relates to dialkyltriazene-bearing estrogens and anti-estrogens that are suited for use as chemotherapeutic drugs for treating carcinomas of the sexual organs of humans and animals.
CN103505741A Tegafur-layered double-metal hydroxide nanometer hybrid modified with polyethylene glycol derivative on surface and preparation of nanometer hybrid The invention discloses a tegafur-layered double-metal hydroxide nanometer hybrid modified with polyethylene glycol monomethyl ether sulfate on the surface (abbreviated to TF-LDH-MPS) and a preparation method of the nanometer hybrid. The invention aims to provide a method as follows: using the tegafur (TF) intercalated LDH (TF-LDH) nanometer hybrid as a model system, using the polyethylene glycol derivative (PEG) polyethylene glycol monomethyl ether sulfate (MPS) with pretending invisibility as a modifier to prepare the MPS modified TF-LDH nanometer hybrid. The nanometer hybrid can be used for improving the dispersion stability and the pretending invisibility of the tegafur-layered double-metal hydroxide, and improving targeted transport and controlled release effects of tegafur, so that the pharmaceutical effect is improved, and the toxic and side effects of the drug are reduced, and the like.
CN103599090A Multi-layer drug sustain-release nano fiber membrane and preparation method thereof The invention discloses a multi-layer drug sustain-release nano fiber membrane and a preparation method thereof. The inner layer and outer layer of the multi-layer membrane are both composed of a polymer A nano fiber with a good biological compatibility, and the middle layer is a drug-carrying nano fiber which is prepared by blending curcumin (CM) and a polymer B with a good biological compatibility. The preparation method comprises the following steps: dissolving the polymer A into a solvent, subjecting the polymer A to an electrostatic spinning process so as to prepare the inner layer, then subjecting a mixed solution of the polymer B and CM to an electrostatic spinning process, continuously depositing the mixed solution on the inner layer so as to obtain the middle layer, finally subjecting the polymer A to an electrostatic spinning process for a second time, and continuously depositing the polymer A on the middle layer so as to obtain the outer layer. The membrane preparation method is simple, can effectively relieve the burst release phenomenon in the early release stage, and can control the drug release by changing the thickness of the polymer A. Taking polymer A-polylactic acid (PLA), and polymer B-cellulose acetate (CA) as an example, the in vitro drug release test results have shown that the drug release rate of the multi-layer drug-carrying membrane is both less than that of a single layer drug loaded membrane no matter after 1 hour or after 240 hours.
US20080063702 Liposomal Formulations Comprising an Amphipathic Weak Base Like Tempamine for Treatment of Neurodegenerative Conditions The present invention provides the use of an amphipathic weak base having defined characteristics for the preparation of a pharmaceutical formulation for the treatment or prevention of neurodegenerative conditions. Preferably, the amphipathic weak base is encapsulated in a liposome. The invention also provides pharmaceutical formulations and methods of use thereof for the treatment or prevention of neurodegenerative conditions. A specific and preferred amphipathic weak base is tempamine (TMN). Further, preferably, tempamine is loaded in sterically stabilized liposomes (SSL-TMN).
US20080293769 Polymorphs of a C-Met/Hgfr Inhibitor This invention relates to polymorphs of (R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to compositions including such salts and polymorphs, and to methods of using such compositions in the treatment of abnormal cell growth in mammals, especially humans.
WO2008019065A1 Use of 3- (4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment of mantle cell lymphomas The treatment, prevention or management of mantle cell lymphomas by administration of an immunomodulatory compound of the invention known as Revlimid® or lenalidomide are disclosed. The invention further relates to the use of this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy for the claimed treatment. Pharmaceutical compositions and single unit dosage forms suitable for use in the invention are also disclosed.
US20110229581 Releasable cationic lipids for nucleic acids delivery systems The present invention is directed to releasable cationic lipids and nanoparticle compositions for the delivery of nucleic acids and methods of modulating an expression of a target gene using the same. In particular, the invention relates to cationic lipids including an acid labile linker, and nanoparticle compositions containing the same.
WO2010025931A3 Pharmaceutical combination of 3- (3-dimethylamino-1-ethyl-2 -methyl-propyl) - phenol and an antiepileptic The present invention relates to a combination comprising as components (a) at least one 3-(3-Dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said combination as well as a method of treating pain, e.g. neuropathic pain, wherein components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.
WO2010037050A2 Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels- Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl- containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
CN1977838A Pharmaceutical use of senkyunolide A, and medicinal composition containing it and its prepairng method The present invention provides medicinal application of cnidium officinale lactone A, medicine composition containing said cnidium officinal lactone A and their preparation method. Said cnidium officinal lactone A has the functions of increasing volume of blood flow of brain, reducing vascular resistance of brain and inhibiting thrombosis, so that it can be used for curing cerebrovascular disease.
WO2008066064A1 Regulation of the activity of transcriptional factor stat by zinc ion To prevent and treat a disease induced by the hyperactivation of STAT by providing a novel STAT activity regulator. Namely, an STAT activity regulator and a preventive/remedy for a disease induced by the hyperactivation of STAT which contain a substance capable of elevating the intracellular zinc concentration, and a method of screening a substance having an effect of regulating the STAT activity are provided.
WO2007111806A2 Cyclopentane heptanoic acid compounds for reducing body fat The present invention relates to compositions, such as bimatoprost, latanoprost and travoprost, and methods to reduce fat in the body of an individual, for example, by topical administration, injection, and/or implantation of such compositions.
US7381411 Preventing influenza virus cell binding; schizophrenia; diagnosing chronic viral disease associated with cancer development Glycoconjugates, therapeutic compositions containing the glycoconjugates and therapeutic methods of using the glycoconjugates are disclosed. In particular, peptide constituents of aglyco 10B, which are immunogenic epitopes responsible for recognition of antigens by the immune system are provided. These glycoconjugates are useful in prevention of influenza virus binding to cells, treatment of schizophrenia and diagnosing chronic viral disease associated with development of cancer.
EP1087775B1 Preventing cerebral infarction through administration of adp-receptor antiplatelet and antihypertensive drugs in combination A method is provided for preventing a cerebral infarction by administering to a patient a combination of an ADP-receptor blocking antiplatelet drug, such as clopidogrel, in combination with an antihypertensive agent such as an angiotensin AII antagonist (for example, irbesartan), an ACE inhibitor (for example, fosinopril) or a NEP/ACE inhibitor such as omapatrilat.
CN1594319A Process for extracting ginkgolide, ginkgolide injection and process for preparing same The invention discloses a process for extracting ginkgolide, ginkgolide injection and process for preparing same, wherein the extracting process consists of disintegrating the ginkgo leaves, leaching by diluted acetone solution, recovering acetone, removing impurities, extracting and purifying with acetic ether, removing impurities with sodium acetate again, reclaiming acetic ether, recrystallizing in ethanol or methanol, filtering, low temperature drying, solubilizing the bilobalide with hydroxypropyl-beta-cyclodextrin to obtain the bilobalide injection.
US20090131380 Novel pharmaceutical composition for topical treatment of skin psoriasis and the treatment method thereof The present invention provides the combination of topical 3,3,′5,5′-tetraiodothyroacetic acid and betamethasone for the treatment of skin psoriasis results in a better outcome than the combination of topical calcipotriol and betamethasone. The present invention also provide a method for treatment of skin psoriasis by using the composition of 3,3,′5,5′-tetraiodothyroacetic acid and betamethasone.
WO2005032519A1 Buccal, polar and non-polar spray containing zolpidem Buccal aerosol sprays or capsules using polar and non-polar solvents have now been developed which provide zolpidem for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation aqueous polar solvent, zolpidem, and optional flavoring agent; formulation II: aqueous polar solvent, zolpidem, optionally flavoring agent, and propellant; formulation III: non-polar solvent, zolpidem, and optional flavoring agent; formulation IV: non-polar solvent, zolpidem, optional flavoring agent, and propellant; formulation V: a mixture of a polar solvent and a non-polar solvent, zolpidem, and optional flavoring agent; formulation VI: a mixture of a polar solvent and a non-polar solvent, zolpidem, optional flavoring agent, and propellant.
WO2009073146A2 Use of immunomodulatory compounds for the treatment of transverse myelitis, multiple sclerosis, and other disorders Methods of treating, preventing or managing transverse myelitis, multiple sclerosis, and/or other disorders are disclosed. The methods encompass the administration of an immunomodulatory compound provided herein, such as 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl-piperidine-2,6-dione or 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindoline. Further described are methods of treatment using the immunomodulatory compounds in combination with a second active agent. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.
CN101948475A Isoflavone derivate-chromene (chroman) oxazines compound, preparation method and application thereof The invention belongs to the technical field of medicines and discloses a series of isoflavone derivate-chromene (chroman) oxazines compounds the general structure of which is shown in the specification, wherein the specific meaning of each substituent group is given in the specification. The invention also provides a preparation method and an application of the compound. The compound has preferable antitumor activity.
CN103341035A Radix bupleuri lipid-lowering soup The invention provides radix bupleruri lipid-lowering soup, which comprises the following components in parts by weight: 60-10 parts of radix bupleruri, 12-15 parts of radix paeoniae rubra, 12-15 parts of radix paeoniae alba, 6-10 parts of finger citron, 6-10 parts of prepared pinellia tuber, 10-15 parts of rhizoma alismatis, 10-15 parts of raw fleece-flower root, 10-15 parts of semen cassiae torae, 6-10 parts of prepared rhubarb, 15-20 parts of the root of red rooted saliva, 10-20 parts of raw hawthorn fruit, 10-15 parts of lotus leaf, 6-10 parts of rhizoma polygonati, and 5-10 parts of schisandra fruit. The radix bupleruri lipid-lowering soup provided by the invention has reverse effects at different degrees on mild and moderate fatty liver with various symptoms, and has therapeutic effects on some hyperlipidemia, particularly triglyceride or low density lipoprotein increase.
US20080300293 Combination of an dpp-iv inhibitor and a ppar-alpha compound The invention relates to a combination which comprises a DPP-IV inhibitor and at least one further PPARα compound, preferably selected from the group consisting of fenofibrate, micronized fenofibrate, bezafibrate, gemfibrazil and ciprofibrate for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of conditions mediated by DPP-IV and PPARα, in particular diabetes, more especially type 2 diabetes mellitus, conditions of IGT, conditions of impaired fasting plasma glucose, metabolic acidosis, ketosis, arthritis, obesity, dyslipidemia and osteoporosis.
WO2011149046A1 Therapeutic agent for pancreatic cancer The inventors have found that excellent therapeutic effects on pancreatic cancer can be achieved by administering an IL-6 inhibitor and an antimetabolite to a pancreatic cancer patient. It is also found that reduction of metastasis from human pancreatic cancer and elimination of ascites are also possible by the administration of an IL-6 inhibitor and an antimetabolite.
WO2008099805A1 Central circulation-improving agent Disclosed is a vasodilator which can specifically improve the central circulation including retinal circulation. Specifically disclosed is a central circulation-improving agent comprising an EP2 receptor agonist as an active ingredient.
CN102125554A Mycobacterium secreted protein new inhibitor The invention provides a mycobacterium secreted protein new inhibitor. In the invention, mycobacterium may be mycobacterium tuberculosis or mycobacteria smegmatis.
CN103054889A Antineoplastic application of Hederagenin-3-O-arabinopyranoside The invention relates to application of hederagenin-3-O-arabinopyranoside (hederagenin-3-O-arabinopyranoside). The Hederagenin-3-O-arabinopyranoside is obtained by utilizing a chemical extraction separation method. The chemical compound structure of the hederagenin-3-O-arabinopyranoside is identified by utilizing physical constants and spectroscopy methods to carry out an antineoplastic pharmacological testing for the hederagenin-3-O-arabinopyranoside, a result shows that the hederagenin-3-O-arabinopyranoside has good effect on antineoplastic aspects ,especially has good effects on restraining human breast cancer cells, sarcoma cells, gastric carcinoma cells, hepatoma carcinoma cells and prostate cancer cells. The hederagenin-3-O-arabinopyranoside can be used for preparing medicines for curing breast cancer, solid tumor, gastric cancer, liver cancer and prostate cancer.
US20110257100 Inhibitors of Protein Tyrosine Kinase Activity This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.
US20120220650 Functional microbially fermented tea extract containing polyphenol derivative and method for producing the same A functional microbially fermented tea extract containing a novel polyphenol derivative and a method for producing the same are provided. A functional microbially fermented tea extract containing various extracts and a novel polyphenol derivative is produced by subjecting, to an extraction treatment, a microbially fermented tea leaf obtained by culturing one species selected from Aspergillus sp. (PK-1), Aspergillus oryzae (NBRS 4214) sp. (AO-1), Aspergillus awamori (NBRS 4122) sp. (SK-1), and Eurotium sp. (KA-1) with a tea leaf. Furthermore, for example, a functional fermented tea extract enriched with a novel polyphenol derivative is produced.
US20080146607 heterocyclic ketones such as (3-Benzyl-pyrrolidin-3-yl)-(1H-indol-5-yl)-methanone, used as antidepressants or anxiolytic agents Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
US20110312934 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine derivatives, preparation thereof, and therapeutic application thereof The invention relates to 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives of the general formula (I) where: R2 is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-4-alkyl, C1-4-alkyloxy-C-M-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl>C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-alkyl, C1-4-fluoroalkyl group; R3 is a hydrogen atom or a substituent selected from halogen atoms and the C1-3 alkyl, —NR4R5, hydroxyl or C1-4 alkyloxy groups; A is a C1-7-alkylene group optionally substituted by one or two Ra groups; B is a C1-7-alkylene group optionally substituted by one or two Rb groups; L is either a nitrogen atom optionally substituted by an Rc or Rd group or a carbon atom substituted by an Re1 group and an Rd group or by two Re2 groups; Rd is a group selected from a hydrogen atom or a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkylthio-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, C1-6-fluoroalkyl, hydroxy-C1-6-alkyl group; Rf is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl, C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-allyl, C1-6-fluoroalkyl or benzyl group. The invention also relates to a method for preparing same and to the therapeutic application thereof.
CN102499924A Application of porphyrin modified by diethylene triamine pentaacetic acid or ethylene diamine tetraacetic acid or ethylene diamine tetraacetic acid The invention discloses an application of porphyrin modified by diethylene triamine pentaacetic acid or ethylene diamine tetraacetic acid or ethylene diamine tetraacetic acid, which has a structure shown below. Experiments show that the porphyrin modified by the diethylene triamine pentaacetic acid or the ethylene diamine tetraacetic acid or the ethylene diamine tetraacetic acid has good therapeutic effects during photodynamic therapy of a prostatic hyperplasia model of a rat.
US20120225875 Heteroarylaminoquinolines as tgf-beta receptor kinase inhibitors Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
WO2013044793A1 High-purity heparin benzyl ester salt, preparation method therefor and application thereof The present invention relates to a high-purity heparin benzyl ester salt, and a preparation method therefor and an application thereof. Specifically, in the present invention, the preparation method of the heparin benzyl ester salt comprises: a heparin benzyl ester quaternary ammonium salt, or a material containing a heparin benzyl ester quaternary ammonium salt, or a heparin benzyl ester salt containing a quaternary ammonium salt reacting with an alkali metal or an aqueous solution of an alkaline-earth metal salt; adding the product of the reaction into a solvent in which the heparin benzyl ester metal salt or the alkaline-earth metal salt is insoluble, and obtaining the heparin benzyl ester salt after precipitation and separation. The heparin benzyl ester salt is featured by high purity, a small amount of residual quaternary ammonium salt, and a simple preparation method. The heparin benzyl ester salt is easily applied in industrial production, can be used for preparing high-purity heparin with a low molecular weight, and has a high yield.
WO2011065800A3 Pyrimidine derivative, method for preparing same and pharmaceutical composition containing same A pyridimine derivative compound of the present invention can be usefully used in bone formation during the growth period as well as in prevention and treatment of metabolic bone diseases such as osteoporosis as a result of increasing bone density by promoting differentiation of osteroblasts. In addition, a pharmaceutical composition of the prevent invention can be used as a therapeutic agent for various metabolic bone diseases such as renal osterodystrophy, osteromalacia, Paget's disease, anostosis, and the like. The pharmaceutical composition also treats fracture and can be used as a therapeutic agent that suppresses bone metastasis of cancer.
CN102058849B Application of Tibetan medicine composite to preparing alcohol withdrawal medicines The invention discloses application of a Tibetan medicine composite to preparing alcohol withdrawal medicines. The Tibetan medicine composite comprises the following raw materials in parts by weight: 5-15 parts of lamiophlomis rotate, 2-10 parts of whin, 15-60 parts of turmeric, 7-20 parts of wild pepper, 5-15 parts of cornu bubali, 15-40 parts of myricariagermanica, 0.1-2.5 parts of red flower, 0.1-5 parts of borneol and 0.1-5 parts of camphor. In the invention, the further research on the pharmacology of the Tibetan medicine composite finds that the Tibetan medicine composite can take an alcohol withdrawal effect effectively through regulating the balance between Chiba and Peigen in a human body. The Tibetan medicine composite comprises purely natural wild medicinal materials grown in Qinghai-Tibet Plateau, contains no stabilizing agents synthesized chemically, has no toxic or side effect on human bodies, is safe and effective and suitable for all people.
US20110071161 Triazolopyridine carboxamide derivatives, preparation thereof and therapeutic use thereof The invention relates to the triazolopyridine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
CN102924621A Mesona chinensis benth polysaccharide and preparation method and applications thereof The invention discloses a method for preparing mesona chinensis benth polysaccharide. The method comprises the following steps that mesona chinensis benth herb is dried and crushed to obtain mesona chinensis benth herb powder, and the mesona chinensis benth herb powder is mixed with 1.0-2.0 percent of sodium carbonate water solution, and then the mixture is extracted at the temperature of 93-97 DEG C for 1.3-1.7 hours and then is filtered; the obtained filtrate is decolored with 10 percent of hydrogen peroxide at the temperature of 45-55 DEG C, and the decolored filtrate is ultrafiltered and purified by 10 K hollow fiber membrane tubes; and the ultrafiltered and purified filtrate is added into absolute ethyl alcohol with 70 percent of filtrate volume, then is centrifuged at the temperature of 4 DEG C and the rotating speed of 5,000rpm after 2-8 hours, sediment is collected and is subjected to freeze drying, and finally the mesona chinensis benth polysaccharide is obtained. The mesona chinensis benth polysaccharide obtained by the method has a radiation-proof effect.
EP1501511A1 Methods of treatment of glaucoma and other conditions mediated by nos-2 expression via inhibition of the egfr pathway Therapeutic methods and compositions for the treatment of glaucoma and other conditions mediated at least in part by the expression of NOS-2 are provided.
WO2011158655A1 Use with utilization of soluble klotho-, fgf23- and fgfr-complex formation mechanism in calcified tissue Provided are a method for screening an agent for controlling calcification, to which signal transduction relates, common to hard tissue and/or blood vessel; a calcification controlling agent; a method for examining calcification of a bone, calcification of a blood vessel and the pathological advance of a disease accompanying the same; and an examination kit therefor. The method for screening an agent for controlling calcification of hard tissue and/or blood vessel according to the first aspect comprises a step for, in a specimen in the absence and presence of a test compound, contacting soluble Klotho with FGFR and FGF23, and a step for selecting a compound causing a change in the specific signal transduction. The calcification controlling agent according to the second aspect comprises a compound capable of inhibiting or promoting the formation of a soluble Klotho-containing complex. The method for examining calcification according to the third aspect comprises a step for measuring the concentration of soluble Klotho, etc. The kit for examining calcification according to the fourth aspect contains a ligand having binding affinity to soluble Klotho, etc.
WO2012147861A1 Composition for inhibiting endoserine-1 production and composition for promoting cell proliferation Provided is a composition for inhibiting endoserine-1 production, a skin-whitening composition, a composition for promoting cell proliferation, and a composition for improvement of wrinkles and sagging, which comprise as the active ingredient thereof a compound represented by general formula (1) or general formula (5).
US6939550 Storage stability An antihistaminic syrup is stabilized against degradation of the active ingredient, by the addition of and about 0.05 to about 5 mg/mL of an aminopolycarboxylic acid such as a salt of ethylenediaminetetraacetic acid.
CN101637475B Application of paederoside acid or plant extract containing same The invention discloses application of paederoside acid shown as a formula 1 or a plant extract containing the same in medicaments in preparing anti-influenza A virus. The compound and the plant extract containing the same have the obvious anti-influenza A virus activity, and have obvious effects of treating influenza A or influenza A viral pneumonia.
CN102125568A Medicinal composition containing clopidogrel and aspirin and application thereof to preparation of medicaments for treating acute non-disabling cerebrovascular diseases The invention discloses a medicinal composition containing clopidogrel and aspirin. The medicinal composition is characterized by comprising the clopidogrel and the aspirin serving as active ingredients, wherein the medicinal composition is prepared in the dose unit that every unit dose of preparation contains 75mg of active ingredients; and both ingredients exist in a free state or pharmaceutically acceptable salt forms. The invention discloses application of the composition to preparation of medicaments for treating an acute non-disabling cerebrovascular disease. The invention has the advantages that: 1, a patient can be easily and conveniently treated by using an oral medicament and has high compliance; and 2, compared with single use of aspirin, the technical scheme of the invention is of great benefit to the patient with the acute non-disabling cerebrovascular diseases without increasing the bleeding rate.
EP2767276A1 Improving / prophylactic agent for chronic kidney disease Problem to be Solved An agent for ameliorating chronic kidney disease which is not an existing symptomatic therapeutic drug for chronic kidney disease, and which can increase the eGFR value and can improve renal function per se is provided. Solution An agent for ameliorating and/or preventing chronic kidney disease containing 5-aminolevulinic acid (ALA) or a derivative thereof, or a salt thereof as an active ingredient is prepared. Preferably, a metal-containing compound such as sodium ferrous citrate is contained in these ALAs. As the above-mentioned ALAs, ALA; various esters such as ALA methylester, ALA ethylester, ALA propylester, ALA butylester, and ALA pentylester; and hydrochlorides, phosphates, and sulfates, and the like of these ALA esters can be preferably exemplified.
CN103169651A Injection containing docetaxel and preparation method of injection The invention discloses an injection containing docetaxel and a preparation method of the injection and belongs to the field of medicinal preparations. Compared with the prior art, a rotary evaporation method is utilized for removing absolute ethyl alcohol added during dosing in the preparation process of the injection, the production time is obviously shortened, the production efficiency is improved, the labor cost and the energy cost are reduced, the stability of a docetaxel injection is greatly improved simultaneously, and the injection has good popularization and application values.
US20090099141 Compositions and methods for treating vitamin d deficiencies The present invention provides for: (a) an oral dosage of vitamin D3 for humans sufficient to maintain a serum level above a minimally sufficient level and below a toxic level when administered according to a schedule of at least one dosage a week up to at least one dosage a day, (b) methods for administering the oral dosages and (c) a kit involving a blister pack and a plurality of oral dosages with instructions for administering the dosages and a location on the blister pack for recording information related to the administration of each dosage, the name of the person receiving the dosages and additional relevant information.
WO2013126799A1 Compositions and methods for ocular delivery of a therapeutic agent Embodiments of various aspects described herein are directed to silk-based compositions for ocular delivery of at least one active agent, e.g., at least one therapeutic agent and methods of using the same. In some embodiments, the silk-based compositions can provide sustained release of at least one therapeutic agent to at least a portion of an eye. Thus, some embodiments of the silk-based compositions can be used for treatment of an ocular condition, e.g., age-related macular degeneration.
US20100260747 Use of Tetrahydrobiopterin as a Marker and a Therapeutic Agent for Fabry Disease Blood and tissue markers of the metabolic status, risk of health complications in Fabry disease patients and as a biomarker to follow the efficacy of treatment in animal models and patients with Fabry disease comprising tetrahydrobiopterin (BH4), precursors and metabolites of BH4, and other related co-factors is disclosed herein. The present invention further describes the use of BH4 therapy as a treatment option for Fabry disease to prevent, slow or reverses vascular cardiac and renal manifestations of Fabry disease.
US20100130577 Pyrazalone derivative formulations Pyrazolone derivative formulations are provided. The formulations include a pyrazolone derivative active agent, e.g., edaravone, and an amphiphilic solubilizing agent. Also provided are methods of making and using the subject formulations.
WO2013016499A1 Methods for preparation of thiophene compounds A method of preparing Compound (1): or a pharmaceutically acceptable salt thereof includes: a) reacting Compound (A) with 3,3- dimetylbut-l-yne in the presence of one or more palladium catalysts selected from the group consisting of Pd(PPh3)4 and Pd(PPh3)2Cl2, and one or more copper catalysts selected from the group consisting of Cul, CuBr, and CuCl, to generate Compound (B); b) treating Compound (B) with an acid to generate Compound (C): c) reducing the cyclohexanone of Compound (C) to cyclohexanol to generate Compound (D); and d) reacting Compound (D) with a base to generate Compound (1), wherein Compounds (A), (B), (C), and (D) are each as depicted herein.
US20050101585 Cannabis-1 (CB1) receptor antagonists; for treatment/inhibiton of drug induced obesity in juveniles/adolescents The use of selective CB1 receptor antagonistic compounds for treating and/or inhibiting CB1 receptor related diseases in juvenile patients (pediatric treatment), e.g. in particular obesity in juvenile patients, and/or for the treatment and/or inhibition of drug induced obesity in juvenile as well as in adolescent patients, and for the manufacture of pharmaceutical compositions for such purposes.
WO2014004854A1 Induction of estrogen receptor beta by cholesterol biosynthesis inhibitors and methods of treatment of cancer Disclosed herein are methods and compositions related to the discovery that cholesterol inhibitors induce the anti-proliferative protein, estrogen receptor beta (ERβ), in both ERα- positive and ERα-negative breast cancer cell lines, including triple negative cells.
US20120004261 Mif modulators The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.
EP1609505A1 Uses of fluorinated triazoles for treaing pain and affective or attention disorders The present invention relates to the use of fluorinated triazoles in treating neurophatic pain and affective and attention disorders including bipolar mood disorders.
US20110312998 Methods of Making and Using Stable Pharmaceutical Compositions Comprising Ketotifen and Naphazoline Stable compositions comprising ketotifen or a ketotifen salt and methods of preparing such compositions are provided. The pH of the compositions remains at less than about 5 during storage. The methods comprise preparing pharmaceutical compositions comprising ketotifen or a ketotifen salt, and adjusting their pH to less than 5, thus slowing the changes of the active ingredients.
US20100226990 Method of Producing Porous Microparticles A method of preparing porous microparticles comprises the steps of combining one or more organic compounds with a volatile system, and drying the system thus formed to provide substantially pure porous microparticles of the organic compound or composite porous microparticles of combinations of organic compounds. Organic compounds used in the method may be one or more of a bioactive, a pharmaceutically acceptable excipient, a pharmaceutically acceptable adjuvant or combinations thereof. The invention also relates to porous microparticles produced by such a method, and pharmaceutical compositions comprising such porous microparticles.
US20100069392 Combination of HMG-COA Reductase Inhibitors with Phosphodiesterase 4 Inhibitors for the Treatment of Inflammatory Pulmonary Disease The invention relates to the combined use of a PDE4 inhibitor with a HMG-CoA reductase inhibitor for the preventive and curative treatment of an inflammatory pulmonary disease.
CN103585171A Aztreonam composition freeze-dried powder for injection The invention provides an aztreonam composition freeze-dried powder for injection, relating to the technical field of drugs and drug preparation. The aztreonam composition freeze-dried powder comprises the following raw material components in parts by weight: 9.47-11.58 parts of aztreonam, 4.74-5.79 parts of chitosan nanoparticles and 75.79-92.63 parts of water for injection. The aztreonam composition freeze-dried powder has the advantages: (1) a composition composed of aztreonam and chitosan nanoparticles according to the proportion of 1:0.5 not only can be used for improving the solubility of aztreonam in water, but also can be used for shortening the dissolving time of aztreonam so as to be beneficial for clinical application; (2) the composition can be used for remarkably enhancing the antibacterial effect of aztreonam and can be used for clinically reducing the dosage and adverse reaction of aztreonam, and an in-vitro experiment proves that 0.2g of aztreonam containing the chitosan nanoparticles has the same antibacterial effect with 0.4g of aztreonam not containing the chitosan nanoparticles; (3) the chitosan nanoparticles can be used as a freeze-dried skeleton agent of the freeze-dried powder for injection to replace arginine, so that the activation effect of arginine to human bodies is eliminated.
CN102212613A Application of (E,E)-2-(phenylmethyl aminocarbonyl)-3-styrene-acrylonitrile and derivatives thereof The invention provides application of (E,E)-2-(phenylmethyl aminocarbonyl)-3-styrene-acrylonitrile and derivatives thereof. The compounds serve as Bcl-2 family protein inhibitors, and play a role of killing tumor cells by directly bonding Bcl-2 and/or Mcl-1 and/or Bcl-xl proteins. The compounds can be used for screening the tumor cells which can be induced for apoptosis, and can be also used for preparing anti-tumor drugs such as the Bcl-2 family protein inhibitors or Bcl-2/Bax and/or Bcl-xL/Bak and/or Mcl-1/Bak protein dimer regulators.
WO2011124992A1 Substantially pure strontium ranelate Provided herein is an improved, commercially viable and industrially advantageous process for the preparation of strontium ranelate, and its intermediates, in high yield and purity. Provided further herein is a highly pure strontium ranelate substantially free of impurities, and pharmaceutical compositions comprising highly pure strontium ranelate substantially free of impurities.
US20080269348 Novel Arylbicyclo[3.1.0]Hexylamines And Methods And Compositions For Their Preparation And Use The invention provides novel arylbicyclo[3.1.0]hexylamines, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.
CN102727515A Medicinal preparation for treating dermatophytosis The invention relates to a medicinal preparation for treating dermatophytosis. The medicinal preparation comprises vitamin C and medical soda which is sodium bicarbonate or sodium carbonate. Through synergism of effects of the drugs, the medicinal preparation can cure dermatophytosis by being used only 2-3times and has a low treatment cost.
CN1606981A Use of phentolamine mesylate as therapeutic agent of feminine sterility Said invention relates to the medical use of leucinocaine phentolamine of treating female infertility, which can be used in external form of suppository, jelly agent and effervesce tablet, and oral taking form of all body administration.
CN102641240A Kukoamine B salt injection and preparation method thereof The invention discloses a kukoamine B salt injection and a preparation method thereof. The preparation for injecting, which takes kukoamine B salt as an active ingredient, contains active-ingredient kukoamine B salt and pharmaceutically acceptable adjuvants such as a stabilizer, a solubilizer and a solvent. The preparation is stable and controllable in quality, safe and effective, and applicable to medicaments for treating pyemia.
WO2014071512A1 Combination therapy and methods for the treatment of respiratory diseases The present disclosure relates to novel combination comprising a homopiperazinium compound having the formula (I): wherein J is a counter ion,; and one or more agents for treating or preventing the pulmonary diseases, for use and method for the treatment or prevention of respiratory diseases. Also provided are novel compounds and intermediates as well as processes for preparing same.
CN1634065A Sustained releasing tablet of buspirone hydrochloride The invention relates to a buspirone slow release tablet for stabilizing mood and improving sleeping, which comprises by weight portion buspirone hydrochloride 15-30g, poly(e-caprolactone) 0-36g, methyl hydroxypropylcellulose 0-270g, carbomer0-54g, the invention can increase the biological availability by 1.66 times.
EP1558240B1 Hypoestoxides, derivatives and agonists thereof for use in the treatment and prophylaxis of hyperlipidemia Methods for treatment and prophylaxis of hyperlipidemias, including hypertriglyceridemia and hypercholesterolemia, are provided. The methods include administering to a host a therapeutically or prophylactically effective amount of a diterpene compound, such as a hypoestoxide.
US20080063682 treatment of surgical adhesions, keloid; continuously controlled release a therapeutic agent in combination with a fucoidan Compositions and methods involving administration of agents useful for the treatment, prevention, inhibition, etc., of inflammatory disease or fibrous adhesions using low sulphate fucans and, if desired, one or more other anti-inflammatory disease or anti-fibrous adhesion agent.
US20130115201 Fluid Supplement with Prenatal Vitamins A fluid supplement is provided that is specifically tailored to meet the health and nutritional needs of a pregnant woman and her developing fetus. The fluid supplement also combats the symptoms of nausea and vomiting that are commonly associated with pregnancy. The fluid supplement contains vitamins, minerals, dietary supplements, and flavor-enhancing ingredients in amounts that safely provide health and nutritional benefits to both the woman and her developing fetus. By using the fluid supplement, a pregnant woman is able to obtain the health and nutritional benefits in a single dose of a palatable fluid supplement instead of having to swallow multiple pills per day.
EP1157000B1 Branched chain amino acid-dependent aminotransferase inhibitors and their use in the treatment of diabetic retinopathy The present invention is directed to a method for the prophylactic and therapeutic treatment of diabetic retinopathy. The method involves the administration of an inhibitor of formulae (I), (II) and (III) of the branch chain amino acid-dependent aminotransferase (BCAT) pathway to an animal, such as a mammal, in particular a human, in an amount sufficient to treat the retina for diabetic retinopathy prophylactically or therapeutically. The present invention is also directed to several novel inhibitors of formula (IV) of the BCAT pathway. In formulae (I-IV), n, m, X and R1-R13 have the meanings given in the description.
CA2565186A1 Substituted thiophen-carboxylic acid amides, the production and the use thereof in the form of a drug The invention relates to novel substituted thiophen-2-carboxylic acid amides of general formula (I), wherein A and R1 to R8 are defined as specified in the claim 1, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, in particular the salts thereof which are physiologically compatible with inorganic or organic acids or bases and exhibit interesting properties.
US20060002919 15625 receptor, a novel G-protein coupled receptor The present invention relates to a newly identified receptor belonging to the superfamily of G-protein-coupled receptors. The invention also relates to polynucleotides encoding the receptor. The invention further relates to methods using the receptor polypeptides and polynucleotides as a target for diagnosis and treatment in receptor-mediated disorders. The invention further relates to drug-screening methods using the receptor polypeptides and polynucleotides to identify agonists and antagonists for diagnosis and treatment. The invention further encompasses agonists and antagonists based on the receptor polypeptides and polynucleotides. The invention further relates to procedures for producing the receptor polypeptides and polynucleotides.
CN101143868A Aldose reductase inhibitor structure and use The present invention discloses the structure of a class of hydantoin type aldose reductase inhibitor and applications. The compound structure provided by the present invention is shown as the formula on the right, the inhibitory activity can be applied to the synthesis of aldose reductase inhibitors (ARIs) and the research on the inhibitory function of aldose reductase, the compound provided by the present invention can be used as an aldose reductase inhibitor to be applied to the treatment of diabetes complications, and can be widely applied in the fields of chemical biology, biomedicine and biological engineering.
CN102440946A Preparation method of dyclonine ointment The invention discloses a preparation method of a dyclonine ointment, and belongs to the field of pharmacy. The invention uses dyclonine, chloroform, stearic acid, paraffin, hydroxybenzoate and yellow soft paraffin as raw materials; dyclonine is a main drug; chloroform is solvent; stearic acid has emulsification effect; paraffin is a matrix of the ointment; hydroxybenzoate is used as a bacteriostatic preservatives; and yellow soft paraffin is used as a backing material. A finished product is prepared through three reactions. The product has advantages of simple process, low raw material price, good effect and convenience for batch production, etc., and can be used for pain relieving and itching relieving of burn, scratch, insect bite, hemorrhoid, ulcer, bedsore and itching dermatopathy and has good effects of relieving pain and itching and sterilizing.
US20100099658 Di(arylamino)aryl compound The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.
US20050059627 Administering antisense oligonucleotides against the mRNA of corticotropin releasing factor subtype-2 (CRF2) receptor; treating anxiety, obsessive-compulsive disorder, panic disorders, post-traumatic stress, phobias and depression This invention relates to antisense oligonucleotides directed against the mRNA of the corticotropin releasing factor subtype-2 (CRF2) receptor which substantially reduce expression of CRF2 receptors in the rodent brain and the use of antisense oligonucleotides in in vivo CNS studies of gene function and to treat a wide range of psychiatric disorders including anxiety, obsessive-compulsive disorder, panic disorders, post-traumatic stress disorder, phobias and depression.
US7576078 Tetrahydroquinoline analogues as muscarinic agonists The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
CN101683370A American ginseng prescription for treating nephritis The invention relates to an American ginseng prescription for treating nephritis. The prescription comprises the following components in percent by weight: 3-5% of American ginseng, 3-5% of bird's nest, 3-5% of Phymatodes crentopinnata (Clarke) Ching, 80-85% of chicken soup and 5-10% of rock candy. The prescription is prepared by the following steps: cutting the American ginseng into shreds, swelling the bird's nest, washing the Phymatodes crentopinnata (Clarke) Ching, crashing the rock candy, putting into the chicken soup altogether and stewing with slow fire for 120 minutes. The prescriptioncan be taken twice one day, the soup is for drinking, and the ginseng and the bird's nest are for eating.
CN103553957A Colchicine derivative containing histone deacetylase inhibitory activity, preparation method and application thereof The invention provides a colchicine derivative that is shown as general formula I and contains histone deacetylase inhibitory activity, its pharmaceutically acceptable salts, a preparation method and application thereof. In the general formula I, X can be carbonyl, methylene, substituted methylene, ethylidene and substituted ethylidene; Y can be an aromatic ring, a substituted aromatic ring, a heteroaromatic ring and a substituted heteroaromatic ring; and Z can be hydrogen, an aromatic ring, a substituted aromatic ring, a heteroaromatic ring and a substituted heteroaromatic ring. The compounds have good anti-tumor activity, and can be applied by means of oral administration, intravenous injection, intramuscular injection and the like clinically.
EP2397138A1 Method of inhibiting C-KIT kinase A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a ompound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
CN102302582A Compound preparation for reinforcing spleen to promote digestion of children and preparation method thereof The invention discloses a compound preparation for reinforcing the spleen to promote digestion of children. The compound preparation is prepared from the following raw material drugs: hawthorn, fresh sea-buckthorn fruits, zinc gluconate, cane sugar and dextrin. The compound preparation disclosed by the invention is used for zinc-deficiency patients of 1-7 years old children or is used for treating anorexia, pica, recurrent aphthous ulcer, upper respiratory tract infection and other symptoms caused by spleen deficiency and dyspepsia. The compound preparation has the advantages of good clinical curative effect, high healing rate and no toxic or side effect.
WO2008093303A3 Method for decreasing inflammation and stress in a mammal using glucose antimetaboltes, avocado or avocado extracts The present invention is directed to a method for decreasing inflammation and stress in a mammal comprising; administration to a mammal a composition comprising a glucose antimetabolite; and wherein said composition comprises amounts of the glucose anti-metabolite sufficient to lower a level of a C-reactive protein in the blood of the mammal subsequent to administration of the glucose anti-metabolite.
US20120114661 Methods of identifying infectious disease and assays for identifying infectious disease Methods of identifying infectious disease infection prior to presentation of symptoms, assays for identifying genomic markers of infectious disease, and methods for diagnosing the underlying etiology of infectious disease.
WO2011022393A3 Phosphatidylcholine transfer protein inhibitors This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.
US6841545 Heat resistance; anticancer drug The present invention relates to a sterile, stable dosage forms suitable for reconstitution and parenteral administration to a patient, said dosage form comprising an amorphous aminoalkyl dihydrogen phosphorothioate, and of amifostine in particular. The invention further relates to a method of preparing such a dosage form, which typically exhibits enhanced thermal stability as compared to existing vacuum dried amorphous amifostine.
US20070254008 Antibiotic formulation and method of treatment A formulation comprised of particles which may be in groups and are comprised of a biocompatible polymer and an antimicrobial drug for controlled release of the drug is disclosed. The particles may be in an aqueous solution comprising thrombin and be dispersed in a gel. The formulation is administered to an area such as an open wound having an orthopedic implant therein and provides a therapeutically effective level of drug to the patient over therapeutically effective period of time.
WO2005012543A2 Quantitative method for detecting yessotoxins in fish products based on the activation caused by the toxin in cellular phosphodiesterase and therapeutic usefulness of said activation The invention relates to a quantitative method for detecting yessotoxins in fish products based on the activation caused by the toxin in cellular phosphodiesterase and therapeutic usefulness of said activation. The cellular target of yessotoxin (YTX) and analogues is the activation of phosphodiesterases (PDEs). The PDEs-YTX union emits a measurable signal. The union can be quantified by means of an affinity biosensor or fluorescence. The biosensor detects bimolecular interactions and makes it possible to determine the presence of YTX due to its interaction with PDEs. Plate fluorescence makes it possible to determine variations in the speed of degradation of fluorescent derivative anthranyloil-AMPc. The speed with which the PDEs degrade this molecule increases in the presence of YTX. The YTX inhibits the immunological activation of rat mastocytese and induces a cytotoxic effect in human hepatocarcinoma cells, which provides two therapeutic utilities of YTXs as anti-allergic and anti-tumoral compound.
CN103068844A Retinol-modified collagen, method for producing same, and external composition for skin containing same Disclosed is a compound which exhibits a higher effect of preventing wrinkle formation, a higher effect of improving wrinkles, a higher effect of making the skin beautiful, and a higher effect of improving skin quality than conventional retinol and retinol derivatives in a sustained manner. Further disclosed are a method for producing the same, and an external composition for the skin and a sheet-shaped cosmetic each containing the same as an active ingredient. More specifically disclosed are retinol-modified collagen in which a dicarboxylic acid is attached to at least one hydroxyl group of collagen and retinol is attached to a carboxyl group of at least one attached dicarboxylic acid, a method for producing the same, and an external composition for the skin and a sheet-shaped cosmetic each containing the same as an active ingredient.
US20090054412 Treatment of Sleep Disorders A method for treating various types of insomnia is provided using 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5methyl-4,5-dihydro-imidazol[1,5,-a][1,4]benzodiazepine-6-one or its pharmaceutically acceptable salt.
US20090214605 Hydrophilic Core Polymeric Micelles for the Delivery of Water-Soluble Compounds The present invention describes the preparation of reverse polymeric micelles (RPM) through hydrophobically-modified star-shaped polyols. More specifically, RPM are obtained from polymeric structures where the polyol constitutes the hydrophilic domain while the hydrophobic shell is obtained either through the modification of existing chemical functions (e.g. esterification) or through copolymerization with hydrocarbon (alkyl)acrylate derivatives. Hydrophilic guests can be accommodated in the micelle core opening new avenues for the use of such carriers as delivery agents for polar active compounds.
WO2008156174A1 Pyrazinamide compound Disclosed is a pyrazinamide compound represented by the formula (1), a tautomer, stereoisomer or pharmaceutically acceptable salt thereof, or a solvate of the compound or the tautomer, stereoisomer or pharmaceutically acceptable salt thereof, which has an excellent GK-activating activity and is therefore useful as a medicinal agent. (1) wherein R1 represents a hydrogen, a C1-8 alkyl group, a C3-8 cycloalkyl group, a C2-9 heterocyclyl group, a phenyl group, a C1-9 heteroaryl group, a C7-14 arylalkyl group or the like; R2 represents a C1-8 alkyl group, a C2-9 heterocyclyl group, a phenyl group, a C1-9 heteroaryl group or the like; Ar represents a monocyclic or fused polycyclic C1-9 heteroaryl group represented by the formula (2) or a C2-9 heterocyclyl group; Y represents -S-, -O- or -NH-; and Z represents -S-, -O- or -CH2-.
WO2013059548A1 Compositions and methods for treating cancer using jak2 inhibitor Compositions, kits, and methods of treating patients with cancer are provided, wherein the methods comprise administering to the patient an effective amount of a JAK2 inhibitor or a JAK2 inhibitor and an IL-6 antagonist, wherein the patient has a cancer or is at risk of developing a cancer that involves IL-6 signaling.
US20120251510 Agents for promoting tissue regeneration by recruiting bone marrow mesenchymal stem cells and/or pluripotent stem cells into blood It was revealed that the intravenous administration of HMGB-1 and S100A8 promoted the healing of skin ulcer by recruiting bone marrow-derived cells to the site of skin ulcer. Furthermore, when HMGB-1 was intravenously administered to cerebral infarction model mice after creation of cerebral infarction, bone marrow-derived cells expressing nerve cell markers were detected in their brain. A marked cerebral infarct-reducing effect was observed in mice intravenously administered with HMGB-1 as compared to the control. The post-cerebral infarction survival rate was increased in the intravenous HMGB-1 administration group. The involvement of bone marrow pluripotent stem cells in the process of bone fracture healing was assessed using mice, and the result demonstrated that bone marrow-derived cells distant from the damaged site migrated to the bone fracture site to repair the damaged tissue.
WO2008032105A3 Flavonoid derivatives and their uses A compound having: a bicyclic ring structure that comprises two fused six-membered carbon rings, wherein one of the rings is aromatic, and wherein one carbon in the bicyclic ring structure may optionally be replaced with a nitrogen, sulfur or oxygen, the bicyclic ring structure being substituted with an optionally substituted pendent aromatic ring, wherein the compound includes one or more acidic substituent group selected from sulfate, sulfonate, phosphate and carboxylate; and pharmaceutically acceptable salts, solvates and pro-drugs thereof. The compounds, pharmaceutically acceptable salts, solutes or pro-drugs thereof, may be used for the treatment of inappropriate angiogenesis, for example in the treatment of cancer, diabetic retinopathy, arthritis, psoriasis, atherosclerosis, macular degeneration, or hemangioma.
US7078418 e.g., 2,6-bis(1-aziridino-1-hydroxyiminomethyl)pyridine; treating colon, stomach, lung, breast and uterus cancer Described are new 1-aziridino-1-hydroxyiminomethyl derivatives with the general formula (I), wherein R is able to is a single bond or a linker moiety capable of covalently bonding two aziridine oxime groups, R1 and R2 independently of one another are selected from the group consisting of —H, —CH3, —C2H5, —CN, —COOH, —COOCH3, —COOC2H5, —CONH2, or —C6H5 group, and n is the whole number 2, provided that R1 and R2 are not both —H and provided that R1 is not —H if R2 is —CH3 and R1 is not —CH3 if R2 is —H The compounds of general formula (I) show antitumor activity.
CN101015563A Intravenous injection microemulsion preparation of teniposide This invention relates to a formulation and preparation method of micro emulsion of Teniposide for intravenous injection. The micro emulsion comprises active components and auxiliary materials, wherein the active components are Teniposide or mixture of Teniposide, paclitaxel, and etoposide; and auxiliary materials is composed of vegetable oil, emulsifying agent or assistant emulsifier, and organic solvent. The micro emulsion for intravenous injection is obtained by preparing active components and auxiliary materials to pre-concentration liquid and adding to 5% glucose solution for clinical use. The invention has the advatages of convenient adminstration, high bioavailability, and reduced toxic anaphylaxis.
US20120178769 Novel compounds for inhibiting eef-2 kinase activity The present invention discloses novel compounds for inhibiting eEF2 kinase and methods of use thereof.
US20080242637 Binding efficiency;cyxicity; therapy for lung, colon, ovariers tumor The present invention relates to a novel drug target in cancer therapy. More closely it relates to use of the cytochrome P450 enzyme CYP2W1 and its promoter as a drug target for cancer therapy. It also relates to screening methods for obtaining therapeutic agents for cancer therapy and to therapeutic agents comprising moieties showing binding affinity for CYP2W1 and moieties with cytotoxic/anti-cancer effect.
CN101780086A Composition of cefperazone sodium and sulbactam sodium and lysine The invention belongs to the technical field of medicine, in particular relates to a composition of cefperazone sodium and sulbactam sodium and lysine, and also provides a preparation method of the composition injection and an application of the composition for preparing drugs of the infectious diseases caused by beta-lactamase bacteria which resists cefoperazone but is sensitive to the composition.
WO2007051390A1 The use of eriocalyxin b in the manufacture of medicaments for treating leukemia The use of eriocalyxin B in the manufacture of medicaments for treating leukemia , wherein the leukemia include leukemia containg AML1-ETO fusion protein , acute promyelocytic leukemia , acute myelocytic leukemia and lymphocytic leukemia . Eriocalyxin B increases the level of peroxidate and influences the phosphorylation and degradation of IκBα to prevent NF-κB from getting into the nucleus in order to inhibition NF-κB pathway . Eriocalyxin B can decrease the phosphorylation of ERI1/2 and inhibit MAPK pathway . Eriocalyxin B can extend the life span of mice and decrease tumor volume in mice model of C57 leukemia and tumor transplantation .
US20100048467 Cystine-Knot Fold Cytokine This invention relates to a novel protein (INSP002), herein identified as a secreted protein that is a member of the Dan family of the cystine-knot fold cytokine superfamily and to the use of this protein and nucleic acid sequences from the encoding genes in the diagnosis, prevention and treatment of disease.
EP2627335A1 Composition for skin treatment A composition comprising from 10 to 15 % by weight of sucrose palmitate. The composition can be used to treat eczema.
CN1977957A Method for preparing toothache drops The present invention relates to a liquid medicine for curing toothache. Said liquid medicine has the functions of promoting blood circulation, relieving inflammation, dispelling wind and stopping pain, so that it can be used for curing various toothaches. Besides, said invention also provides its preparation method.
WO2010075663A1 A formulation of silymarin with high efficiency and prolonged action and the preparation method thereof A formulation of silymarin with high efficiency and prolonged action and the preparation method thereof are disclosed. Said formulation consists of a solid dispersion of silymarin, silicon dioxide nanoparticles of silymarin, sustained-release matrix materials and release accelerator, wherein the mass ratio of the solid dispersion, nanoparticles, matrix materials and accelerator is 1: 0.5~1.25: 0.1~0.3: 0.1~0.3. The drug loading rate of the nanopartiles of silymarin is 51.95-52.87%. The solid dispersion comprises silymarin, polyvidone K30, soybean phospholipid, acrylic resin IV in the mass ratio of 1: 1~3: 0.3~0.8: 0.2~0.5.
CN1947718A Cucurbitacin dispersion tablets and its prepn. method A dispersing tablet of cucurbitacin with high disintegrating speed and solubility is proportionally prepared from cucurbitacin, lactose, starch, microcrystalline cellulose, carboxymethyl starch sodium, cross-linked polyvinyl pyrrolidone, magnesium stearate, superfine silica gel powder, polyvinyl pyrrolidone, sodium laurylsulfate and tween-80 through wet granulating and tabletting.
US20060189656 Piperidine derivatives and agent comprising the derivative as active ingredient Piperidine derivatives represented by formula (I) or nontoxic salts thereof (wherein symbols are defined in the description): Since the compound represented by formula (I) has a PDE4 inhibitory activity, it is useful for preventing and/or treating inflammatory diseases, diabetic diseases, allergic diseases, autoimmune diseases, osteoporosis, bone fracture, obesity, depression, Parkinson's disease, dementia, ischemia-reperfusion injury, leukemia and the like.
EP1335917B1 Condensed pyridoindole derivatives Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents. In particular, the invention relates to compounds that, are potent and selective inhibitors of cyclic guanosine 3', 5'-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5, ad have utility in a variety of therapeutic areas wherein such inhibition is considered beneficial, including the treatment of cardiovascular disorders and erectile dysfunction.
WO2007092026A1 Dipyridamole extended-release formulations and process for preparing same The invention is directed to a dipyridamole formulation comprising an extended release formulation of dipyridamole and a pharmaceutically acceptable carboxylic acid, wherein the formulation is in a tablet solid form having a diameter of about 1.5 mm to about 3 mm. Optionally, the formulation may further comprise an immediate release acetylsalicylic acid formulation.
CN103275105A Azasugar thiazine alkane ketone derivative, synthetic method and application thereof in medicinal preparation The invention discloses an azasugar thiazine alkane ketone derivative, and simultaneously provides a synthetic method of the derivative and application in medicinal preparation. The azasugar derivative can be used as intermediate raw material for synthesizing compound with anti-HIV virus activity, and the synthesis preparation method of the provided azasugar thiazine alkane ketone derivative comprises the following steps: using partially protected azido sugar as initial raw material, transiting azido into aza Wittig reagent by Staudinger, and then opening the sugar ring, generating epimino by reaction of free aldehyde group and aza Wittig reagent, and then forming a ring with a mercaptoacetic acid and obtaining a double ring products with partial hydroxy protected, and finally obtaining the object product by removing the protective group, obtaining the pure product of the compound isomer by column chromatography separation, and the obtained compound isomer has a good anti-HIV virus activity and can be applied in preparation of anti-HIV virus medicinal preparation.
CN102935109A Compound crossostephium chinense tablet The invention relates to a compound crossostephium chinense tablet. The compound crossostephium chinense tablet is characterized in that ingredients and matching ratio of the compound crossostephium chinense tablet are as the follow. The nine drugs are porphyrized according to the matching ratio and mixed evenly to form tablets or capsules. 1.5-2k of compound crossostephium chinense tablets is taken orally each time and three times a day, and the compound crossostephium chinense tablets are swallowed by using warm water after meal and taken for four to five weeks continuously.
CN102633743A Structure of hydroxyethyl benzisothiazolinone aliphatic ester and bactericidal activity thereof The invention discloses a new benzo (d) isothiazole-3(2H)-ketone compound, and the application of the compound used as active ingredient of bacteriostatic agent. The compound has good bactericidal activity for bacteria such as staphylococcus albus, staphylococcus aureus, bacillus subtilis, colon bacillus, pseudomonas aeruginosa, klebsiella pneumoniae and the like, thus being developed into a novel industrial bacteriacide, agricultural bacteriacide, medical bacteriacide or the like.
US20060166927 Compounds that bind to the interferon-gamma, preparation method thereof and medicaments containing same Compound capable of binding to gamma-interferon (γ-IFN), chosen from the molecules corresponding to formula (I) below: in which X is a divalent spacer group that is sufficiently long to allow the two oligosaccharide fragments A and B to each bind to one of the peptide sequences 125 to 143 of the C-terminal ends of a γ-interferon (γ-IFN) homodimer, n represents an integer from 0 to 10, and for example equal to 0, 1, 2, 3, 4 or 5, and each R independently represents a hydrogen atom, an SO3 − group or a phosphate group, on the condition that no SO3 − group is in the 3-position of the glucosamine units of compound (I). The invention also relates to the process for preparing these compounds, to the complexes formed by these compounds and gamma-interferon, and to the medicaments comprising these compounds or complexes.
US7993673 Fast acting paracetamol formulation containing a small amount of antacid A dosage form such as a swallow tablet or a capsule formulation is described comprising paracetamol, low levels of sodium bicarbonate or potassium bicarbonate or mixtures thereof, and at least one pharmaceutically acceptable excipient.
CN102451213A Liniment for removing bromhidrosis The invention provides a liniment for removing bromhidrosis. The liniment is prepared with the following materials in part by weight: 25 to 40 parts of alumen exsiccatum, 2 to 5 parts of litharge, a moderate amount of ethanol, 1 to 4 parts of borneol, 10 to 15 parts of ammonia, 15 to 30 parts of clam meal, 6 to 12 parts of waxgourd seeds and 3 to 8 parts of essence. The liniment for removing bromhidrosis is applicable to the treatment of bromhidrosis, has the effects of killing and inhibiting bacteria, arresting sweating and preventing complications, and can realize local dryness and sterility to achieve the effects of treatment and prevention. The effect of the liniment is rapid, and the curative effect is remarkable and persistent; and the liniment does not have toxic and side effects, does not injure skin, is safe and convenient to use, and is suitable for people of all ages.
US20090221989 System and method for the prevention and treatment of bacterial and fungal infections including urinary tract infections (uti) using a hypohalous acid composition Disclosed is a system that prevents the development of infection and biofilm establishment in medical devices in general, and in particular Urinary Tract Infections (UTI), including Catheter-Associated Urinary Tract Infections (CAUTI). The system comprises of a medical device (such as a catheter) and an antimicrobial composition containing an antimicrobial compound. A medical device delivers the composition both to the inside and/or outside portions of the device, as well as to the inside of the bladder itself and to the urethra. Reduction or elimination of the infection may be accomplished by irrigating the medical device, bathing the bladder, or irrigating the bladder with the composition.
CA2474211C Antiproliferative quinazolines Quinazoline compounds of Formula I which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.
CN1958568B A kind of compound for preventing or curing infection of helicobacter pylori, preparation method, and application This invention relates to a compound for treating or preventing bacteria infection, especially Helicobacter pylori infection, and accompanied diseases, and its preparation method and medical applications.
US20080107634 Using mix comprising bifidobacterium and lactobacillus as tool in treatment of gastrointestinal and influenzal disorders The object of the present invention is a probiotic bacteria based composition and use thereof in the prevention and/or treatment of respiratory pathologies and/or infections and in the contemporaneous improvement of the intestinal functionality, which can be compromised by therapeutic treatments adopted for re-solving said pathological conditions. Besides that, aim of this invention is a probiotic bacteria-based composition comprising moreover a suitable quantity of at least a substance or nourishment having prebiotic properties and eventually, of suitable pharmacologically active substances.
EP2658550A1 Agonists of toll like receptor for treating cardiovasuclar disease and obesity A method for treating or aiding in preventing cardiovascular disease in a patient, comprising the step of administering to the patient a therapeutically effective amount of an agonist of an endosomal TLR. The agonist of the endosomal TLR may be an agonist of TLR3, optionally poly l:poly C12U or Poly (l:C).
US20120052093 Compositions and methods for preventing and treating uterine disease The present invention relates to methods and compositions for preventing and treating uterine disease, and in particular to vaccines and bacteriophage compositions for treating or preventing puerperal metritis, clinical endometritis and/or subclinical endometritis.
WO2010065069A3 Compositions comprising renin-angiotensin aldosterone system inhibitors and lipoic acid compounds, and the use thereof for the treatment of renin-angiotensin aldosterone system related disorders Compositions are provided which can be useful in treating a renin-angiotensin aldosterone system-related disorder. These compositions include renin-angiotensin aldosterone system inhibitors and lipoic acid compounds, as well as other therapeutic agents, and are useful in treating hypertension, stroke, metabolic syndrome, or other renin-angiotensin aldosterone system-related disorders in a subject. The compositions are also useful in improving vasodilation, reducing proteinuria, and reducing insulin resistance in a subject. Pharmaceutical compositions and methods of treatment using the compositions are further provided.
WO2005032540A1 Remedy for respiratory diseases comprising n-(benzoyl)amino acid derivative as the active ingredient A preventive/remedy for respiratory diseases characterized by containing a compound represented by the following general formula (I), its optically active form or a pharmaceutically acceptable salt thereof as the active ingredient: (I) wherein Z represents -C(CH3)2- or -CH(CH(CH3)2)-; n is from 0 to 2; R1 represents C1-4 alkyl, hydroxyl, trifluoromethyl or acetoxy; and R2 represents H or C1-4 alkyl. This drug, which aims at achieving an antitussive effect, shows excellent effects as a preventive/remedy for respiratory diseases such as lung caner, common cold syndrome, lung tuberculosis, pneumonia, acute bronchitis and chronic bronchitis.
WO2013111085A1 Pharmaceutical composition for the treatment of erectile dysfunction The present invention concerns a pharmaceutical composition comprising, by way of active substances: - papaverine, or one of the pharmaceutically acceptable salts thereof, and - at least one calcium antagonist from the class of dihydropyridines, or a pharmaceutically acceptable salt thereof; and optionally - at least one nitrated derivative, or a pharmaceutically acceptable salt thereof; optionally in association with at least one pharmaceutically acceptable vehicle or excipient, in particular for the use thereof in the prevention or treatment of erectile dysfunction in a person.
US8697673 Bicyclic pyridinones Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
US20080213398 Modified Azole Compounds as Antifungal and Antibacterial Agents The present invention relates to the compounds of formula (I), their preparation and use as antifungal and/or antibacterial agents. where the values for R1, R2, R3, R4, R5 and A are as defined herein.
WO2008131411A3 Stimulating neuronal growth using brevetoxins Disclosed are methods of treating neurodegenerative diseases or disorders in a subject in need of such treatment. The methods comprise administering to a subject in need of such treatment a therapeutically effective amount of brevetoxin or brevetoxin derivatives. Included in the diseases and disorders are Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, Multiple sclerosis (MS), Amyotrophic Lateral Sclerosis (ALS/Lou Gehrig's Disease) and other Motor Neuron Diseases, Prion Diseases, Frontotemporal Dementia (FTD), and CNS dysfunctions such as schizophrenia, depression, and epilepsy. Also included are neurodegenerations resulting from stroke, heart attack, head and spinal cord trauma, traumatic brain injury, bleeding in the brain and other injuries to the central nervous system (CNS).
US20090076035 Deuterium-enriched paliperidone The present application describes deuterium-enriched peliperidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20110118340 Delivery of rnai constructs to oligodendrocytes The invention provides methods for delivering a double-stranded nbonucleic acid (dsRNA) to the central nervous system of a subject, and particularly, to oligodendrocytes of a subject by localized delivery to the brain, e.g., to the corpus caïlosum. For example, the dsRNA molecules can include a first sequence that is selected from the Sroup consisting of the sense sequences of Tables 8, 10, 13-16, and a second sequence selected from the group consisting of the antisense sequences of Tables 8, 10, and 13-16. The dsRNA molecules can include naturally occurring nucleotides or can include at least one modified nucleotide, such as a 2′-O-methyl modified nucleotide, a nucleotide comprising a 5′-phosphorothioate group, or a terminal nucleotide linked to a conjugate group, such as to a cholesteryl derivative or a vitamin E group. Alternatively, the modified nucleotide may be chosen from the group consisting of a 2f-deoxy-2′-fliιioro modified nucleotide, a 2′-de-oxy-modified nucleotide, a locked nucleotide, an abasic nucleotide, 2′-amino-modified nucleotide, 2′-alkyl-modified nucleotide, morpholino nucleotide, a phosphoramidate, and a non-natural bas comprising nucleotide. Generally, such modified sequences will be based on a first sequence of a dsRNA selected from the group consisting of the sense sequences of Tables 8, 10, and 13-16, and a second sequence selected from the group consisting of the antisense sequences of Tables 8 10, and 13-16.
CN103705527A Vitamin K2 compound for preventing and treating arthritis The invention provides a vitamin K2 compound for preventing and treating arthritis, and belongs to the field of medicine or health-care food formulae. Per 1000g of the compound comprises 0.05-0.25g of vitamin K2, 0.005-0.01g of vitamin D, 500-750g of glucosamine and 499.945-249.740g of solid or liquid matrix. The compound which is mechanically stirred and uniformly mixed under a normal temperature or heating condition is prepared to soft capsules, hard capsules or troches. The medicine or health-care food formed by the formula has remarkable preventing and treating effects on common osteoarthritis of the middle aged or the aged people, especially postmenopausal women.
CA2750265A1 Methods of alleviating or treating signs and/or symptoms associated with moderate to severe parkinson's disease The present invention provides a method for alleviating motor complications and motor indications in a patient suffering from moderate to severe Parkinson's disease by administering a composition which provides an effective amount of the compound of Formula I.
US20090131353 Using cyclic nucleotide phosphodiesterase profiles as tool in detection of cell proliferative disorders The present invention provides diagnostic methods and kits for diagnosis of chronic lymphocytic leukemia (CLL) by determining expression levels of isoforms of cyclic nucleotide phosphodiesterases (PDEs) associated with CLL particularly, PDE7B and/or PDE3B, and a ratio of mRNA expression of PDE7B to PDE3B. The present invention provides that CLL lymphocytes uniformly expressed high levels of PDE7B and low levels of PDE3B relative to those of normal lymphocytes. A method of treatment and a pharmaceutical composition for CLL comprising one or more therapeutic agents capable of modulating expression or activity levels of isoforms of PDEs associated with CLL, and/or reversing the ratio of PDE7B/PDE3B mRNA expression levels are also provided.
US20120251495 Pterin based therapies for inflammatory conditions Disclosed herein are methods for the treatment of cancer and inflammatory-based diseases and disorders, such as hepatitis B virus infection based upon the administration of calcium pterin. In one embodiment is a method of treating cancer comprising administration of dipterinyl calcium pentahydrate (DCP). In another embodiment is a method of treating hepatitis B virus infection comprising administration of dipterinyl calcium pentahydrate (DCP).
CN101559230A Special solvent of lansoprazole lyophilized powder for injection The invention relates to a special solvent of lansoprazole lyophilized powder for injection, comprising sodium chloride, ethylene diamine teraacetic acid or edetate and water for injection, wherein the weight ratio of materials is as follows: 0.5-5% of sodium chloride, 0.01-0.1% of ethylene diamine teraacetic acid or edetate, the rest of water for injection, and the gross is 100%. The preparation process is as follows: sodium chloride, ethylene diamine teraacetic acid or edetate are weighed and put in a vessel, water for injection accounting for 80% of total weight is added to be stirred and evenly mixed, pH value of the solution is adjusted to be 4.0-7.0, water for injection is used for fixing volume to full dose, the solution is filled in an ampoule bottle after being filtered by sand pipe, filter bulb and 0.22mum millipore filtering film, and the special solvent of lansoprazole lyophilized powder for injection is prepared by sealing, sterilizing, quality testing and packaging.
WO2011048148A3 Glycoside derivative and uses thereof This invention relates to compounds represented by formula (I) wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.
EP2687264A1 Macrophage Activating Factor for treatment of endometriosis The present invention relates to methods and compounds for the treatment and prevention of endometriosis and/or symptoms associated with endometriosis in a patient. More particularly, compositions comprising a Macrophage Activating Factor for use in the treatment or prevention of endometriosis and/or symptoms associated therewith are envisaged.
CN103393618A Pharmaceutical composition comprising 11-deoxy-prostaglandin compound and method for stabilizing same Provided is a pharmaceutical composition comprising a 11-deoxy-prostaglandin compound represented by formula (I): and a fatty acid ester. By mixing the compound of formula (I) and a fatty acid ester, the compound of formula (I) will be stabilized
CN103083230A Fructose-containing injection and preparation method thereof The invention relates to a fructose-containing injection and a preparation method of the injection; each 10L of injection contains the following components in proportion: 250-500g of fructose and 0.01-0.05mol of buffer; and the pH (potential of hydrogen) value of the injection is 4.5-5.5. The fructose injection provided by the invention has excellent stability which is higher than the stability in the prior art.
CN103274915A Diterpenoid compounds libertellenone G and libertellenone H with antineoplastic activities and application thereof The invention relates to the technical field of a medicine, and particularly relates to two diterpenoid compounds libertellenone G and libertellenone H with antineoplastic activities extracted from secondary metabolite of arctic curvularia molecular genus. The chemical structural formulas are shown in the specification. The invention also provides a preparation method of the diterpenoid compounds, and application of the diterpenoid compounds in preparation of an antitumor drug.
US20110130435 Time-released medication for applying to crustacean ovarian development A time-released medication for applying to crustacean ovarian development comprises a covering oil and a serotonin-related reagent. The covering oil is coated with the serotonin-related reagent and provides a sustainable releasing effect for the serotonin-related reagent. The serotonin-related reagent is selected from a group of serotonin, a precursor of serotonin, a derivative of serotonin and an agonist of serotonin. The coating relationship between the serotonin-related reagent and the covering oil makes them become a time-released medication.
WO2014054970A1 Solid dosage form having an anorectic effect (variants) The invention relates to the pharmaceutical industry and medicine and can be used in the creation and administration of solid dosage forms for the treatment and/or prophylaxis of obesity. The present invention addresses the problem of creating an effective solid dosage form containing sibutramine hydrochloride monohydrate and having an anorectic effect. The problem of interest is solved by the inclusion of additional mineral substances in the solid dosage form and also by the use of carbon-13 and nitrogen-15 isotopes. The technical results of the invention are: a greater therapeutic effect (a reduction in body weight or a decrease in the rate of weight gain) in the treatment and/or prophylaxis of obesity with no decrease in the duration of the effect or increase in the concentration of sibutramine hydrochloride monohydrate, and a more rapid onset of said therapeutic effect.
CN1911924A Extraction method of Nepal eagle tail isoflavone, its derivative and medicipal composition using said derivative as active component The present invention provides process of extracting Nepal roof iris rhizome isoflavone, novel Nepal roof iris rhizome isoflavone derivative and its medicinal salt. The present invention also relates to the preparation process of the derivative, medicinal composition with the derivative as the active component, and the application of the derivative and medicinal composition in preparing medicines for improving and treating cardiac and cerebral vascular diseases and osteoporosis.
US7723390 Thyroid hormones or their salts in capsule or in swallowable uniform soft-gel gelatin matrices for treatment of hypothyroidism The present invention provides for pharmaceutical formulations based on thyroid hormones enabling a safe and stable oral administration in the framework of the strict therapeutic index prescribed in case of thyroid disorders.
CN101418293A Tiny RNA-21 antisense oligonucleotides and use thereof The invention relates to antisense oligonucleotide of micro RNA-21 and application thereof. After the antisense oligonucleotide AMO-miR-21 acts on Raji cells, the cell growth is inhibited, the apoptosis is increased obviously, and the intracellular expression level of microRNA-21 is reduced significantly. The antisense oligonucleotide can be used for preparing drugs for preventing or treating cancers, in particular for preparing the drugs for preventing or treating blood system related to tumors (such as lymphoma).
WO2008000513A3 Peptide compounds for the treatment of hyperexcitability disorders and diseases associated with ion channel dysfunction The present invention is directed to the use of a class of peptide compounds for treating diseases associated with hyperexcitability. The present invention is also directed to the use of a class of peptide compounds for treating diseases associated with dysfunction of an ion channel.
EP0728209B1 Endothelin-converting enzyme The invention relates to endothelin-converting enzymes containing the polypeptide sequence described in SEQ. ID. NO. 30 or SEQ. ID. NO. 36 or functional fragments thereof, genes which code for such enzymes, and processes for producing the said enzymes and the use thereof.
WO2005090340A1 Piperidine-1-carboxamide derivative Disclosed is a compound represented by the following general formula (I): (I) [wherein Ar1 represents an optionally substituted aryl group or heteroaryl group; R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 independently represent a hydrogen atom, a hydroxyl group, a lower alkyl group, an aralkyl group or an aryl group; T, U, V and W independently represent an optionally substituted methine group or a nitrogen atom and at least one of them represents a methine group; X represents a single bond, a methylene group or an ethylene group; and Y represents a single bond or a group expressed as -O-, -C(R1)(R2)-, -O-C(R3)(R4)-, -C(R5)(R6)-O- or -C(R7)(R8)-C(R9)(R10)-]. This compound is useful as an agent for the treatment of various diseases associated with NPY.
EP1071419B1 Cannabinoids as antioxidants and neuroprotectants Cannabinoids have been found to have antioxidant properties, unrelated to NMDA receptor antagonism. This new found property makes the cannabinoids useful in the treatment and prophylaxis of wide variety of oxidation associated diseases, such as ischemic, age-related, inflammatory and autoimmune diseases. The cannabinoids are found to have particular application as neuroprotectants, for example in limiting neurological damage following ischemic insults, such as stroke and trauma, or in the treatment of neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease and HIV dementia. Nonpsychoactive cannabinoids, such as cannabidoil, are particularly advantageous to use because they avoid toxicity that is encountered with psychoactive cannabinoids at high doses useful in the method of the present invention. A particular disclosed class of cannabinoids useful as neuroprotective antioxidants is formula (I) wherein the R group is independently selected from the group consisting of H, CH3, and COCH3.
US20120251579 Compositions for generating an antigen specific immune response The present invention provides for the purposeful utilisation of the induction of senescence in eukaryotic cells for induction of an antigen specific immune response. Such cells can be normal cells, pre-malignant and malignant cells as well as virally or bacterially infected cells, for the generation of an immune response, preferably a cellular or humoral immune response comprising T-cells and/or B-cells, whose immune response is directed specifically against antigens from those cells in which senescence was induced and then comprises an immune response against the senescent cells itself as well as to the non-senescent counterparts harbouring the same antigens.
US7674898 Anhydrous crystal of β-lactam compound and method for preparation thereof The present invention provides anhydrous crystals of β-lactam compound represented by the formula: The β-lactam compound of the invention is produced by heating an aqueous solution of a salt of the β-lactam compound and adjusting the pH of the aqueous solution to 3 or lower. The β-lactam compound has excellent storage stability.
CN103054800A Flurbiprofen acetaminophen resin lipid microsphere injection, freeze-drying lipid microsphere injection and preparation methods The invention relates to a flurbiprofen acetaminophen resin lipid microsphere injection, a freeze-drying lipid microsphere injection and a preparation method. Through a reasonable composition proportion and a preparation process with controllable parameters, good stability and strong operability, the flurbiprofen acetaminophen resin which is an indissolvable drug is wrapped in an oil phase and an interfacial film of a lipid microsphere, so that not only is the solubility of the drug remarkably strengthened, but also precipitation and oxidation do not occur easily, the physical and chemical stabilities of the drug are greatly improved, the devitrification phenomenon is avoided in the use and storage processes, a slow release effect is exerted and the action time of the drug in the blood plasma is prolonged, meanwhile, as the lipid microsphere targets to an inflammation part, the toxicity and the vessel stimulation during injection are remarkably reduced, the clinical application of the injections is safer, the treatment effect is more remarkable, and the injections and the methods are suitable for industrialized production and clinical application.
CN102775291A Emodin derivative and application thereof in preparing antibacterial agents The invention relates to an emodin derivative and application thereof in preparing antibacterial agents. The chemical structural formula of the emodin derivative is represented as formula (I), wherein R1, R2, R3 and R4 are -F, -Cl, -Br, -I or -NO2; and R5, R6 and R7 are -H, -CH3, -CH2CH3 and -COCH3. The emodin derivative is a high-activity compound designed by performing structural modification on compounds with natural emodin as a matrix according to the principle of medical molecules. Experiments prove that the emodin derivative has good effects of resisting drug-resistance bacteria and superbacteria, the pharmaceutical effect of the emodin derivative is remarkably better than that of the emodin, and a new choice is provided for clinical medication.
WO2005099685A1 Liquid external preparation containing sodium cromoglycate [PROBLEMS] To provide a liquid external preparation capable of relieving both of pain and itch occurring at affected parts, such as ocular part and nasal cavity, because of sodium cromoglycate. [MEANS FOR SOLVING PROBLEMS] There is provided a liquid external preparation comprising sodium cromoglycate and a mucopolysaccharide.
WO2006068075A1 Peroxisome proliferator-activated recepotr ϝ ligand It is intended to provide a peroxisome proliferator-activated receptor Ϝ (PPARϜ) ligand originating in a natural material and a composition for preventing or ameliorating insulin resistance syndrome, diabetes, obesity or obesity of the visceral fat type characterized by containing the ligand as the active ingredient. Namely, a PPARϜ ligand which contains, as the active ingredient, at least one compound selected from the group consisting of coumaperine and its derivatives; and a composition for preventing or ameliorating insulin resistance syndrome, diabetes, obesity or obesity of the visceral fat type characterized which contains the above compound as the active ingredient.
CN101200465A Decahydronaphthalene compounds and medical uses thereof The invention discloses a compound in the formula I. The compound can be used to prepare TNF Alpha, IL-1 Beta or iNOS expression inhibitor and NF-Kappa B activity inhibitor, and also used to prepare the drug for the treatment or the prevention of the autoimmune diseases, the tumor or the arteriosclerosis.
WO2006011159A3 Stabilized pharmaceutical composition containing rabeprazole sodium with improved bioavailability The present invention relates to stable pharmaceutical composition of rabeprazole sodium in a form of enteric coated pellets, either alone or in combination with one or more prokinetic agent, preferably mosapride in a form of sustained release tablets, in a single unit dosage form, which provides enhanced bioavailability of rabeprazole. Present invention also discloses process for preparation of said pharmaceutical formulation.
CN103655566A Application of compound in preparation of medicine for preventing and treating glaucoma The invention discloses new application of three compounds and similar compounds or medicinal salt thereof in preparation of medicine for preventing and treating glaucoma through lowering intraocular pressure. The compound has very remarkable effect in preventing and treating glaucoma through lowering intraocular pressure.
US20090124549 administering to a patient infected with mycobacterium tuberculosis, a therapeutically effective amount of an isolated polypeptide ( a polypeptide covalently linked to a carrier); protective immune response Methods for producing an immune response to Mycobacterium tuberculosis (Mtb) are disclosed herein. In several examples, the immune response is a protective immune response. In additional embodiments, methods are disclosed for preventing an infection with Mtb, or treating an infection with Mtb. Pharmaceutical compositions for the prevention and/or treatment of tuberculosis are also disclosed.
WO2007061783A1 Treatment and prevention of bone loss using resolvins The present invention provides new methods for inducing or promoting bone growth and/or for reducing or preventing bone deterioration in a mammal subject. The inventive methods generally comprise administering to the subject an effective amount of a resolvin. In particular, the inventive methods may be useful for treating or preventing conditions associated with bone degradation, deterioration or degeneration such as periodontal disease, osteoarthritis, and metastatic bone disease and osteolytic bone disease. Pharmaceutical compositions and kits comprising at least one resolvin are also provided that can be used to performed the inventive methods.
US7074406 Treating allergic diseases with humanized anti-CD40L antibody The present invention is directed to humanized antibodies which bind human gp39 and their use as therapeutic agents. These humanized antibodies are especially useful for treatment of autoimmune diseases.
CN1559432A Medicine for treating infantile enterorrhea A medicine in the form of powder, instant particles, oral liquid, cream, tablet, or capsule for treating infantal diarrhea is proportionally prepared from sodium alginate, glucomannan and carragheenin.
CN101870768A Polyethylene glycol derivatives of activated lactone compounds The invention relates to polyethylene glycol derivatives of activated lactone compounds, a preparation method thereof, a medicine composition containing the polyethylene glycol derivatives and application of the medicine composition in the aspects of bacteria and eliminating inflammation, killing pains, resisting viruses and the like.
CN102657867A Transcriptional regulator combination The invention relates to a method for treating androgen simulated diseases of a subject through delivering a combination containing an effective dose of I Kappa B kinase subunit alpha active inhibitors to the subject who needs treatment, which can also be used for reducing the risk of prostatic cancer of a subject through delivering the combination to the subject with high risk of prostatic cancer. The invention also relates to a method for recognizing a regulator of I Kappa B kinase subunit alpha regulated transcriptional activity. The invention also relates to a method for determining the I Kappa B kinase subunit alpha regulated transcriptional activity in nonhuman mammal test subjects.
CN101406524A Vaginal lotion for cleaning, disinfecting and preventing diseases The invention discloses clean, sterile and prophylactic vaginal douche, which is prepared by uniform mixing of eucalyptus oil, furacilinum, chlorpheniramine and washing accessory agents such as EDTA sodium, glycerol, flavorless opacifying agent, peppermint and borneol. Raw materials for realizing broad-spectrum antibacterium and inhibting mold and other harmful bacteria and raw materials having pesticidal effect and fragrant scent are prepared into a mixture which is taken as the vaginal douche. The clean, sterile and prophylactic vaginal douche has the advantages that the manufacturing process is simple; the dosage is accurate to control; and the douche has refreshing and fragrant functions besides the functions of cleaning, disinfection, sterilization, antisepsis and so on. People have obvious comfortable and refreshing feeling after using the clean, sterile and prophylactic vaginal douche.
US20100256071 CHD5 encoding nucleic acids, polypeptides, antibodies and methods of use thereof Nucleic acid sequences encoding chromodomain helicase DNA-binding (CHD) proteins, CHD proteins, and antibodies thereto and methods of use thereof are disclosed.
WO2012110425A1 Methods for monitoring the response to treatment and for treating colorectal cancer The present invention relates to a calpain inhibitor for use for delaying or inhibiting the secondary resistance to an anti-cancer agent in a patient suffering from colorectal cancer. The invention also refers to a method for monitoring the response to a treatment of a patient suffering from a cancer chosen from colorectal cancer, gastric cancer, esophageal cancer, non- small-cell and small-cell lung cancers, leukemia, lymphomas, central nervous system maligant gliomas and ovarian carcinomas, and preferably colorectal cancer, comprising: a. treating said patient with an anti-cancer agent for a time period of at least 5 months; then b. measuring the level of expression of at least one gene selected from the group consisting of calpain, annexin A2 and S100A10 genes, in cancer cells of said patient.
WO2008045663A3 Aryl-substituted heterocyclic pde4 inhibitors as antiinflammatory agents Disclosed herein are potent and selective aryl-substituted heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role.
CN102424696A Shikonin amino deoxy glycosides and application thereof in preparation of antitumor medicines The invention discloses shikonin amino deoxy glycosides and application thereof in preparation of antitumor medicines. Experiments prove that: the shikonin amino deoxy glycosides have obvious antitumor activity, IC50 is 0.32-0.88mu g/mL, the antitumor activity is 50 to 100 times that of shikonin, and is higher than or equal to the inhibition of a positive control medicine of amycin to the tested cancer cell strains, the shikonin amino deoxy glycosides are proved to have obvious antitumor effect further through the research of the inhibition to nude mice transplanted tumor with human tumor cell, and the shikonin amino deoxy glycosides have a good prospect for developing clinical antitumor medicines.
US7250407 For the treatment of disorders associated with dyslipoproteinemia, including cardiovascular disease, atherosclerosis, restenosis, hyperlipidemia, and endotoxemia septic shock The invention relates to genetic approaches to supply nucleotide sequences encoding modified forms of the native forms of apolipoprotein A-I (ApoA-I): mature ApoA-I, preproApoA-I and proApoA-I; including native ApoA-I modified to contain ApoA-I agonists, peptides which mimic the activity of ApoA-I; ApoA-I superagonists, peptides which exceed the activity of native ApoA-I; and modified native ApoA-I having one or more amphipathic helices replaced by the nucleotide sequences of one or more ApoA-I agonists; for the treatment of disorders associated with dyslipoproteinemia, including cardiovascular disease, atherosclerosis, restenosis, hyperlipidemia, and other disorders such as septic shock.
US20050222182 Stabilized pharmaceutical compositions of halofuginone and other quinazolinone derivatives The present invention relates to acid stabilized compositions containing as an active ingredient a quinazolinone derivative, preferably halofuginone or a pharmaceutically acceptable salt of halofuginone. More particularly the present invention relates to use of an acid for improving the stability of a topical, parenteral or oral composition containing quinazolinone derivatives as an active ingredient, preferably halofuginone. Surprisingly, even dry solid tablet dosage forms showed improved stability by addition of an acidic component.
CN102526198A Medicine with cinnamon and chromium as additives and preparation method for health care product The invention discloses a medicine with cinnamon and chromium as additives and a preparation method for a health care product. Smashed and screened cinnamon powder and chromium-contained compound are mixed at normal temperature and normal pressure; the above mixture is added into medicines, food and health care products; 88.8-99.9 parts by weight of cinnamon powder and 0.1-11.2 parts by weight of chromium-contained compound are weighed; the chromium-contained compound is chromium picolinate, chromium chloride, chromium nicotinate or chromium yeast. The composition of the cinnamon and the chromium has the functions of regulating blood sugar and preventing and treating diabetes mellitus.
CN101343281A Novel amidino based pyridinyl cephalosporins compound The invention belongs to the medical technique field, particularly relating to hydrates of novel guanyl pyridyl cephalosporin compounds, acceptable salt thereof in pharmacy, easily hydrolysable ester thereof, isomers thereof, hydrate thereof, as well as ester or salt thereof as shown in a general formula (I), wherein , R<1>, R<2>, R<3> and Z are defined in the specification; and the invention also relates to a preparation method of the compounds, a medical composition containing the compounds, and applications of the compounds in preparing medicines for curing and/or preventing infectious diseases.
CN103349668A Application of Polyflavanostilbene A in preparing drug for treating endometrial cancer The invention discloses an application of Polyflavanostilbene A in preparing a drug for treating endometrial cancer, which belongs to the technical field of novel drug use. According to the invention, the in-vitro MTT (Methyl Thiazolyl Tetrazolium) antitumor activity evaluation discovers that the Polyflavanostilbene A also has an obvious inhibiting effect on the growth of human endometrial cancer cell strains ISK and RL95-2. Thus, the Polyflavanostilbene A can be used for preparing an anti-endometrial cancer drug and has good prospects in development and application. The use of the Polyflavanostilbene A in preparing the drug for treating endometrial cancer is disclosed for the first time. The skeleton type is brand-new, and the Polyflavanostilbene A has unexpectedly strong inhibitory activity to the human endometrial cancer cell.
US20110294898 Crystalline Forms of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol Hydrochloride A hitherto unknown crystalline form of (−)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride, pharmaceutical compositions containing the new crystalline form, methods of producing the new crystalline form, and a related method of use including treatment of, e.g., pain and/or urinary incontinence.
WO2011138380A1 Pharmaceutical formulations comprising pioglitazone and linagliptin The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and pioglitazone, processes for the preparation thereof, and their use to treat certain diseases.
US20120028983 Novel compound having 3-heteroarylpyrimidin-4-(3h)-one structure and pharmaceutical preparation containing same Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]
CN103054838A Application of (trans)-3-(3-hydroxy-4-methoxy-phenyl) acrolein and derivative thereof in preparing pharmaceutical composition for preventing and treating bone metabolic disturbance disease The invention provides an application of a compound of formula (I) shown in the specification and a pharmaceutical salt thereof in preparing a pharmaceutical composition for preventing and treating bone metabolic disturbance diseases, wherein in the formula (I), R1 represents hydroxyl or a C1-6 alkyl ester group; and X represents O, NR2, NO or NOOR3, R2 represents H or C1-6 alkyl, and R3 represents C1-6 alkyl. The invention further provides an application of a compound of formula (II) shown in the specification and a pharmaceutical salt thereof in preparing a pharmaceutical composition for preventing and treating bone metabolic disturbance diseases, wherein in the formula (II), R1 represent hydroxyl or a C1-6 alkyl ester group; and n is equal to 1 or 2.
CA2186039C New oral pharmaceutical dosage form An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more antibacterial compounds in a fixed formulation. The fixed formulation is intended for oral use and in the form of an enteric coating layered tablet, a capsule or a multiple unit tableted dosage form. The multiple unit dosage form is most preferred. The new fixed formulation is especially useful in the treatment of disorders associated with Helicobacter infections.
WO2007085036A1 Treatment of friedreich' s ataxia Use of porphyrin compounds comprising a complexed Ca2+, Zn2+ or Mg2+ ion for the production of a pharmaceutical preparation for the treatment of Friedreich' s ataxia or for the treatment or prevention of a disease associated therewith.
CN101543486A Application of tetrahydrocurcumin in preparing antidepressant and method for preparing solid dispersion of tetrahydrocurcumin The invention relates to application of tetrahydrocurcumin in preparing an antidepressant and a method for preparing a solid dispersion of the tetrahydrocurcumin. The invention aims to provide the application of the tetrahydrocurcumin to prepare the antidepressant. The tetrahydrocurcumin and a surfactant are mixed in certain proportion to obtain the solid dispersion of the tetrahydrocurcumin. The method for preparing the solid dispersion of the tetrahydrocurcumin comprises the following steps that: according to the weight ratio of 1:3-1:30, the tetrahydrocurcumin and the surfactant are heated until completely melted, frozen in a low-temperature environment, and taken out, dried and crushed to obtain the solid dispersion of the tetrahydrocurcumin. The tetrahydrocurcumin and the solid dispersion of the tetrahydrocurcumin are used for preparing drugs, health care products, foods or food additives of relieving mental depression. The tetrahydrocurcumin has the function of relieving mental depression, and the function of the tetrahydrocurcumin is possibly related with the influence on a monoamine neurotransmitter system; moreover, compared with fluoxetine, the tetrahydrocurcumin has the advantages of low toxicity and good curing effect.
CN103601789A Neotigogenin compounds as well as preparation method and application thereof The invention relates to neotigogenin compounds with structural general formulas of (I) and (II). The neotigogenin compounds are extracted from a whole herb of C.tuberosum and are {neotigogenin,3-O-beta-D-glucose-(1->2)-[beta-D-glucose-(1->4)]-beta-D-glucose-(1->4)-beta-D-galactopyranoside} (I), and {neotigogenin,3-O-beta-D-glucose-(1->2)-[beta-D-glucose-(1->3)]-beta-D-glucose-(1->4)-beta-D-galactopyranoside (II). The neotigogenin compounds have platelet aggregation induction activity and can be further applied to preparation of in vivo hemostatic drugs, so that the neotigogenin compounds have an important clinical application value.
WO2005000311A1 Substituted diketopiperazines for the treatment of benign prostatic hyperplasia A method of treating or preventing benign prostatic hyperplasia which comprises administering to a mammal in need thereof of an effective amount of a compound of Formula (I) where R1, R2, R3 and R4 are defined as provided in claim 1.
US20080226550 Mercaptan containing diagnostic agents for imaging malignant melanoma and distant metastases and rhenium (186Re, 188Re) therapeutic complexes for treating the same The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tumors, e.g., carcinomas, melanomas and other tumors. In another embodiment, the invention relates to methods of imaging tumors using radiolabeled metal complexes. Preferred radiolabeled complexes for imaging tumors include technetium and rhenium complexes. The high tumor uptake and significant tumor/nontumor ratios of the technetium complexes of the invention indicate that such small technetium-99m-based molecular probes can be developed as in-vivo diagnostic agents for melanoma and its metastases. In yet another embodiment, the invention relates to methods of treatment of tumors using a radiolabeled metal complex as a radiopharmaceutical agent to treat the tumor.
EP2313373A1 Heterocyclic derivatives that are used in the treatment of neurodegenerative diseases The present invention relates to compounds of Formula (I) below, to their pharmaceutically acceptable salts and to their isomers or mixtures of isomers: HetAr−X−CHR1R2 (I) in which: - HetAr represents a group chosen from: - X represents a linear, saturated or unsaturated, hydrocarbon-based chain comprising from 8 to 22 carbon atoms, optionally interrupted by an –NH- or –NH-CO- group, - R1 represents a hydrogen atom or an –OH, -O(C1-C6)alkyl, -OCO((C1-C6)alkyl), -OSO2((C1-C6)alkyl) or –OSO3H group, and - R2 represents a hydrogen atom or a (C2-C6)alkynyl, (C2‑C6)alkenyl or (C3-C6)cycloalkyl group. The present invention also relates to a process for preparing the compounds of Formula (I), and also to the use thereof, especially in the treatment of neurodegenerative diseases.
WO2006125958A1 2-phenyl substituted imidazol [4 , 5b] pyridine/ pyrazine and purine derivatives as glucokinase modulators Compounds of Formula (I), wherein R1- R10, A and X1 to X3 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
US7169775 Amino methyl imidazoles as C5a receptor modulators Amino methyl imidazoles of Formula I are provided: wherein R, R1, R2, R3, R4, R5, and R6 are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.
US20070098777 Pharmaceutical or Food Composition for Treatment or Prevention of Brain Edema Melatonin has an activity of treating or preventing brain edema. Thus, the invention relates to a pharmaceutical composition comprising melatonin as an active ingredient. And, the invention relates to use of melatonin in the preparation of a pharmaceutical composition comprising melatonin as an active ingredient.
US20100143500 Methods and Compositions for Inhibiting GSK-3 In Glial Cell Related Disorders A method of treating a glial cell related disorder in a mammalian subject includes administering a drug which enhances or prolongs GSK-3 α or β inactivation.
US20080004247 Combinations of Statins with Bronchodilators The invention provides medicaments comprising combinations of bronchodilators, glucocorticosteroids and HMG-CoA reductase inhibitors in the treatment of respiratory disorders such as chronic obstructive pulmonary disease (COPD).
US8372837 Pyridone and pyridazone analogues as GPR119 modulators Novel compounds of structure Formula (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R21, T1, T2, T3 and T4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
CN103570669A Brain-targeted O-desmethylvenlafaxine phenolic ester prodrug and preparation method and applications thereof The invention relates to a brain-targeted O-desmethylvenlafaxine phenolic ester prodrug and a preparation method and applications thereof, and discloses a brain-targeted compound in the formula (I), and a preparation method and applications thereof, including the compound in the formula (I) and salts thereof and a preparation method for a drug composition, and applications in treating central nervous system diseases, the R is specially defined in a specification, the compound in the formula (I) is a heteroaromatic substituent-containing 1-[2-(dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclohexanol, (O-desmethylvenlafaxine, ODV) prodrug which is converted into ODV in organisms through metallosim to play a pharmacological action, and is used for treating or aiding treatment of central nervous system diseases such as depression and the like.
US20100285073 a micro-rna family that modulates fibrosis and uses thereof The present invention relates to the identification of a microRNA family, designated miR-29a-c, that is a key regulator of fibrosis in cardiac tissue. The inventors show that members of the miR-29 family are down-regulated in the heart tissue in response to stress, and are up-regulated in heart tissue of mice that are resistant to both stress and fibrosis. Also provided are methods of modulating expression and activity of the miR-29 family of miRNAs as a treatment for fibrotic disease, including cardiac hypertrophy, skeletal muscle fibrosis other fibrosis related diseases and collagen loss-related disease.
WO2007053131A3 Acrylamide derivatives as antibiotic agents The present invention is directed to antibacterial compounds formula (I), wherein, independently for each occurrence, A is a monocyclic ring of 4-7 atoms containing 0-2 heteroatoms, a bicyclic ring of 8-12 atoms containing 0-4 heteroatoms or a tricyclic ring of 8-12 atoms containing 0-6 heteroatoms wherein the rings are independently aliphatic, aromatic, heteroaryl or heterocyclic in nature, the heteroatoms are selected from N, S or O and the rings are optionally substituted with one or more groups selected from CM alkyl, OR', CN, OCF3, F, Cl, Br, I; wherein R' is H, alkyl, aralkyl, or heteroaralkyl; R is formula (II), (III), (IV), (V), (VI), (VII) wherein, independently for each occurrence, R1 is H, alkyl, or aryl, or R1 and R2 taken together form a fused ring; R2 is H, alkyl, or aryl, or R2 and R1 taken together form a fused ring, or R2 and R3 taken together form a spirocyclic ring; R3 is H, alkyl, or aryl, or R3 and R2 taken together form a spirocyclic ring; R4 is H, alkyl, aryl, hydroxy substituted alkyl, or -C(O)ONa; R5 is H, alkyl, or aryl; R6 is H, alkyl, or aryl; and L1 is O or H2.
CN101152511A Medicament for treating hyperthyroidism disease and method of preparing the same The invention relates to a medicine for curing hyperthyroidism and a method of preparing the medicine. The medicine is composed of 10 to 40 portion of fresh yam, 10 to 40 portion of raw oyster, 10 to 40 portion of fortune's drynaria rhizome, 10 to 40 portion of milkvetch root, 10 to 40 portion of pumice, 10 to 40 portion of climbing groundsel herb, 10 to 40 portion of spicaprunellae, 10 to 40 portion of sargassum, 10 to 40 portion of thallus eckloniae, 10 to 40 portion of white mustard seed, 5 to 20 portion of thunberg fritillary bulb, 5 to 20 portion of tuber pinelliak, 5 to 20 portion of angelica, 5 to 20 portion of ampelopsis japonica, 5 to 20 portion of pipewort, 5 to 20 portion of tangshen, 5 to 20 portion of trigone, 5 to 20 portion of rhizoma zedoariae, 2 to 8 portion of cyclophosphamide and 0.3 to 1 portion of tapazole by the weight percent, which are processed through a series of procedures, including medicine selection, drying arrow crushing, sifting arrow sterilization arrow preparation and packaging. The invention is characterized by quick effect, short period of treatment, high therapeutic effect, little toxicity and side effect, convenience in being taken and prevention of recurrence, etc.
CN102743343A Decitabine composition, preparation method thereof, application thereof in medicinal lyophilized preparation, medicinal lyophilized preparation product, and preparation method of medicinal lyophilized preparation product The invention belongs to the field of medicines, especially relates to the field of decitabine preparation, and more especially relates to a decitabine composition, a preparation method of the decitabine composition, an application thereof in a medicinal lyophilized preparation, a medicinal lyophilized preparation product, and a preparation method of the medicinal lyophilized preparation product. The invention aims at providing a decitabine composition and a preparation method thereof. With the decitabine composition, the dissolving speed of decitabine in a preparation process is increased, the stability of a decitabine preparation product is improved, and no organic solvent residue is left in the preparation product. According to the invention, micronized decitabine is adopted as a raw material, and potassium dihydrogen phosphate and sodium hydroxide are adopted as auxiliary materials. With an ultrasonic material dissolving method, the main medicine is dissolved into an emulsion, such that the use of the organic solvent is avoided, and the residue of the organic solvent in the medicine preparation product is avoided. Therefore, the safety of the preparation in clinical application is greatly improved. Also, during a lyophilized preparation production process, lyophilization equipment is prevented from being damaged by the organic solvent.
US20110251133 Blockade of gamma-secretase activity to promote myelination by oligodendrocytes Methods are provided for enhancing myelination. Myelination is enhanced by administration of agents that are inhibitors of γ-secretase. Methods of screening for pharmaceutically active compounds that enhance myelination, and for genes involved in myelination are also provided.
US20100297007 Ligand directed toroidal nanoparticles for therapy and diagnostic imaging The present invention provides nanoparticles, methods of making the nanoparticles, and methods of using the nanoparticles to deliver therapeutic agents and/or imaging agents.
US20110319401 Five crystal forms, methods of preparation, pharmaceutical compositions and applications of xlf-iii-43 This invention discloses that the five crystal forms of XLF-III-43 can be used as crude drugs. The invention also relates to the preparation methods of the five crystal forms of XLF-III-43 as crude drugs, to the applications of the sterling of the five crystal forms of XLF-III-43 and mixed crystals in different proportions as medicinally active components to develop various kinds of medicines and compound medicines. In addition, this invention also relates to applying the crystal samples of XLF-III-43 as crude drugs to treat kidney dysfunction, cardiocerebral vessel diseases, hypertension, type II diabetic mellitus, complications of hypertension and diabetic mellitus, tumor, precancerosis, edema, and achieves therapeutic effects by enhancing blood drug levels resulted from effects of crystal forms in the processes of treating all kinds of diseases.
CN2798943Y Cicatrix plaster The utility model discloses a medicinal plaster for scar, which adopts the principles that the plaster is pasted on an affected part and treatment is carried out by slowly relieving the medicine effect. The utility model comprises a back lining layer used as a plaster base layer, wherein an impermeable layer is pasted on the back lining layer, a plaster adhesive layer is pasted on the impermeable layer, and a protection layer is pasted on the plaster adhesive layer. The utility model has the advantages of convenient, safe and reliable use, no side effect and good curative effect; in addition, the effective ingredients of the medicine are not easy to dissipate, which is favor for the absorption of the affected part. Thereby, the utility model is an ideal medicinal plaster for scar.
US6998403 Antidepressants; N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-1,2-dihydro-3H-benzo[e]indole-3-carboxamide; antagonist of adrenergic receptor, serotonin receptor; anxiety, schizophrenia, Parkinson's disease, cognitive disorders, schizophrenia A compound of formula (I): wherein: R1 and R2 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, and R3 and R4 represent hydrogen, or R1 and R4 represent hydrogen and R2 and R3 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, or R1 and R2 represent hydrogen and R3 and R4 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, addition salts thereof with a pharmaceutically acceptable acid or base, and methods of treating conditions susceptible to α2-AR/5-HT2C antagonists.
US20100189683 Pulsatile Dosing of Gossypol for Treatment of Disease This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.
US20080108692 Alkylene selenocyanate or an alkylene isoselenocyanate moiety; anticancer agents; food supplements; 1,4-phenylenebis(alkylene)selenocyanate A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.
US7879356 AB block polymers, comprising a polylactone part made from monomers such as lactic acid, and B is derived from hydroxyl, amine, or carboxyl terminated compound endcapped with nonreactive group; storage stablity; anti-adhesions The present invention relates to novel bioabsorbable polymeric compositions based upon AB polyester polyether or related diblocks and triblocks. Compositions according to the present invention may be used in medical applications, for example, for reducing or preventing adhesion formation subsequent to medical procedures such as surgery, for producing surgical articles including stents and grafts, as coatings, sealants, lubricants, as transient barriers in the body, for materials which control the release of bioactive agents in the body, for wound and burn dressings and producing biodegradable articles, among numerous others.
WO2008111520A1 Gene related to life extension and use thereof Disclosed is an enhancer of an action of an insulin/IGF-1 signaling system, which comprises a substance capable of inhibiting the expression or activity of WDR6, preferably a substance selected from items (a) to (c): (a) an antisense nucleic acid to a nucleic acid encoding WDR6; (b) a neutralizing antibody directed against WDR6; and (c) a lower-molecular-weight compound having an antagonistic activity on WDR6. Also disclosed is a method for the screening of a substance capable or modulating an activity of an insulin/IGF-1 signaling system, which comprises the steps of: contacting WDR6, a partial peptide thereof or a cell capable of expressing WDR6 with any one of compounds of interest; and selecting a compound which can change the expression or activity of WDR6 or the partial peptide thereof.
CN1989972A Finasteroid oral preparation and method for preparing same The invention relates to a non-finasteride oral preparation and preparation method, specifically which consists of main drug non-finasteride and medicinal findings. Its contents are oily liquid or semi-solid, and it can be made of soft capsules, liquid-filled capsules and oral emulsion. The important contribution of the invention is preparing the steroidal hormone compounds into liquid or semi-solid in agent preparation early period, avoiding occupational hazard caused by dust flying, protecting workers involving in manufacture;In addition, non-finasteride is the combination of lipophilic compounds, oily liquid or semi-solid drugs and supplies, it can increase the drug dissolution rate, improve bioavailability. The application of the invention can improve labor protection, and also can provide better curative effect in clinical application.
US20100113376 Process for dosing self-emulsifying drug delivery systems The present invention provides process for dosing a self-dispersing drug delivery system comprising an active compound, said process comprising the step of using a dosage dispenser to dose a defined amount of said self-dispersing drug delivery system comprising an active compound and a dosage dispenser containing a self-dispersing drug delivery system comprising an active compound.
EP2687524A1 Azole derivative Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where R1 represents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.
CN1966016A Drink for treating infant diarrhea Disclosed is a beverage for treating infantile diarrhea, which is prepared from malt, medicated leaven, haw, green tangerine orange peel, creeping euphorbia, Biden bipinnata, baikal skullcap root, root of herbaceous peony, smoked plum, bamboo leaves, reed rhizome, Chinese yam powder, red date, chicken's gizzard-skin and dried alum through baking treatment and pure water dilution.
US8148378 Pyridazine derivatives and their use as inhibitors of stearoyl-CoA desaturase-1 activity in a mammal A method of treating an SCD-mediated disease or condition in a mammal, preferably a human, includes administering to a mammal a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. The SCD-mediated disease or condition may be selected from the group consisting of Type II diabetes, impaired glucose tolerance, insulin resistance, obesity, fatty liver, non-alcoholic steatohepatitis, dyslipidemia, metabolic syndrome, acne, cardiovascular disease, hypertriglyceridemia, inflammation, cancer, and any combination of these.
US6906081 For treatment of Alzheimer's disease, learning disabilities This invention relates to a method of treating cognition deficit disorders comprising administering to a mammal in need of such treatment an effective amount of a dual histamine H3 receptor antagonist/m2 muscarinic antagonist, or a combination of a histamine H3 receptor antagonist and a m2 muscarinic antagonist.
CN103172606A Coumarin compound with anti-tumor activity The invention relates to a coumarin compound with anti-tumor activity as well as a pharmaceutical composition and applications of the pharmaceutical composition.
CN103239478A Calcium carbonate milk composition freeze-dried orally disintegrating tablets, and preparation method thereof The invention provides a calcium carbonate milk composition, comprising 0.2%-0.8% by weight of calcium carbonate, 1.3%-2.4% by weight of mannitol, 2%-4% by weight of gelatin, 90%-97% by weight of milk powder, 0.1% -0.15% by weight of sucralose. The invention also provides calcium carbonate milk freeze-dried orally disintegrating tablets prepared by the above composition. The freeze-dried orally disintegrating tablets are simple in components, can be taken without water and mastication, can be disintegrated within 2 seconds in a human oral cavity, have few residues in intestinal tracts, can be absorbed completely, have good mouthfeel and are very suitable for being taken by infants.
EP2742026A1 Sweet flavor modifier The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.
WO2011131135A1 Heteroaryl (alkyl) dithiocarbamate compounds, preparation methods and uses thereof Heteroaryl (alkyl) dithiocarbamate compounds represented by general formula (I) or their pharmaceutical salts, their preparation methods and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as antitumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.
US20090209653 Agent for increasing testosterone level Provided is a substance which is a safer and more commonly-consumed food ingredient that increase the testosterone level. The testosterone enhancer of the invention comprises vitamin K as an active ingredient. The vitamin is preferably menaquinone-4 and/or menaquinone-7. This enhancer is useful as pharmaceutical agents, supplements, health foods or functional foods for the prevention, amelioration and/or treatment of a condition or disease induced by the decreased testosterone level.
US20110003861 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives, new pharmacological agents for the treatment of arthritis, cancer and related pain 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives of formula (I) useful as pharmacological agents for the treatment of arthritis, cancer and related pain.
CN101129698B Eye drops containing turmeric extractive and preparation method thereof Disclosed is an eye drop containing turmeric extract which is prepared from the following constituents (by weight ratio): turmeric extract 0. 15-0. 45, taurine 0. 07, sodium hyaluronate 0. 033, vitamin B6 0. 033, boracic acid 0. 8-1. 2, borax 0. 8-1. 2, polyoxyethylene hydrogenated castor oil 1. 5-4. 5 and balancing distilled water. The invention also relates to the process for preparing the eye drop, which contains the precursor of human body hormones, and is capable of facilitating auto-regulated hormones in human body, increasing lacrimal gland secretion, increasing eye cells vitality, improving eye microcirculation, and alleviating symptoms of dry-eye patients.
EP0858337B1 A pharmaceutical composition for the treatment of autoimmune diseases A pharmaceutical composition comprising an anti-inflammatory drug capable of suppressing the production of cytokines (CSAID), an immunosuppressant and a pharmaceutically acceptable excipient.
CN102000091A Bufarenogin, and application of derivatives and pharmaceutically acceptable salts thereof The invention provides a bufarenogin and application of derivatives or pharmaceutically acceptable salts thereof. Results of in vivo and in vitro experiments show that bufarenogin can cause cycle arrest of hepatocarcinoma cells, restrain cell multiplication and induce cell apoptosis. Thus, the bufarenogin, and the derivatives or the pharmaceutically acceptable salts thereof can be used for preparing medicines for treating various tumors, including hepatocarcinoma.
US20100152242 Transdermal Electrotransport Delivery Device Including an Antimicrobial Compatible Reservoir Composition A transdermal electrotransport drug delivery device having an anode, a cathode and a source of electrical power electrically connected to the anode and the cathode. At least one of the anode and the cathode includes an electrode and a reservoir comprised of a housing composed of a polymeric material and an aqueous medium in contact with the housing. The aqueous medium includes (i) a drug or an electrolyte salt or a mixture thereof, (ii) propylene glycol, and (iii) an antimicrobial agent in an amount sufficient to inhibit microbial growth in the aqueous medium. The propylene glycol prevents the antimicrobial agent from being adsorbed by other materials used in the construction of the delivery device. A process for preparing a transdermal electrotransport drug delivery device is also provided.
US20120183600 Novel composition for treating metabolic syndrome and other conditions The invention relates to a composition that includes a first agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5′-monophosphate-activated protein kinase (AMPK) activator; a second agent that possesses anti-inflammatory activity; and a third agent that possesses serotonin activity.
EP1502593A1 The use of Stanozolol for the preparation of anti-inflammatory and anti-degenerative drugs The present invention relates to the use of stanozolol for the preparation of medicaments with an anti-inflammatory and anti-degenerative action which are indicated in human and veterinary medicine for the treatment of disorders with inflammatory and/or degenerative etiological components, including arthritis, osteoarthritis, canine tracheal collapse and neurodegenerative disorders in humans or animals.
WO2009112651A1 Imidazo[1,2-a]pyridine-2-carboxamide derivatives, preparation thereof and application thereof in therapeutics The invention relates to compounds of the formula (I) in which: X and Y define, together with the nitrogen atom bearing them, a saturated or partially saturated monocyclic or bicyclic amino with 5 to 10 links optionally including 1 to 2 additional heteroatoms selected from O, S, N and optionally substituted by a halogen atom, a (C1-C6)alkyl group, a (C1-C6)alkoxy group, cyano, NRaRb, COOR8, the (C1-C6)alkyl and (C1-C6)alkoxy groups being optionally substituted by one or more halogen atoms; R1 is a hydrogen atom, a halogen atom, a (C1-C6)alkoxy group, a (C1-C6)alkyl group; R2 is a hydrogen atom or an optionally substituted (C1-C6)alkyl group, an optionally substituted (C1-C6)alkoxy group, a (C2-C6)alkenyl group, a (C2-C6)alkynyl group, a -CO-R5 group, a -CO-NR6R7 group, a CO-O-R8 group, a -NR9-CO-R10 group, a -N=CH-NraRb group, a halogen atom, a cyano, nitro, hydroxyiminoalkyl, alkoxyiminoalkyl group, a (C1-C6)alkylthio group, a (C1-C6)alkylsulfinyl group, a (C1-C6)alkylsulfonyl group, a (((C1-C6)alkyl)3)silylethynyl group, a -SO2-NR9R10 group, an optionally substituted phenyl group, an optionally substituted heterocyclic group; R3 is a hydrogen atom, a (C2-C6)alkyl group, a (C1-C6)alkoxy group or a halogen atom; R4 is a hydrogen atom, a (C1-C4)alkyl group, a (C1-C4)alkoxy group or a fluorine atom; wherein said compounds are in the form of a base or an addition salt to an acid. The invention can be used in therapeutics.
EP2362770A2 Compositions and methods for treating or preventing radiation injury The invention provides compositions and methods featuring Nrf2 activators for treating or preventing radiation-associated tissue damage.
CN103263396A Meloxicam dispersible tablets and preparation method thereof The invention discloses meloxicam dispersible tablets and a preparation method thereof. The meloxicam dispersible tablets consist of meloxicam, aluminum magnesium silicate and filling agent, wherein the weight ratio of the meloxicam to the aluminum magnesium silicate is 1:(5-20). The preparation method comprises the following steps of: mixing the meloxicam, the filling agent and a part of aluminum magnesium silicate uniformly, performing wet granulation, reshaping granules, adding the rest aluminum magnesium silicate, mixing uniformly and tabletting. The dispersible tablets are quick in disintegration, uniform in dispersion, good in dissolution effect and very wide in application prospect.
WO2014023104A1 Compound with xanthine oxidase inhibitory activity and salt thereof, preparation method and usage for the same Compound with xanthine oxidase inhibitory activity and salt, a midbody, a preparation method, and pharmaceutical composition thereof are provided. The preparation method of the compound is simple and easy to be implemented. The product can be used as an inhibitor of the xanthine oxidase, and used for curing or preventing hyperuricemia or gout disease.
CN102675384A Synthesis method of ent-kaurene type glycoside and biological activities thereof The invention relates to a cheap, practical and feasible synthesis method of synthesizing stevioside into ent-kaurene type glycoside. The structure of the compound is represented as the general formula (I), wherein the definition of R1, R2, X and Y are illustrated in the specification. The invention discloses potential application values and detailed preparation methods of the kind of the compound in the aspects of anti-tumor and anti-inflammation and physical data of Fourier transform infrared spectroscopy (FT-IR), 1H nuclear magnetic resonance (1HNMR), mass spectrum-electrospray ionization (MS-ESI) and the like.
WO2013038740A1 Method for screening for substance or factor capable of promoting muscle hypertrophy The present invention provides: a method for treating muscular atrophy; and a method and a means both for promoting muscle hypertrophy. Specifically, the present invention provides a method for screening for a substance or factor capable of promoting muscle hypertrophy, comprising: (a) a step of measuring the concentration of superoxide and/or peroxynitrous acid and/or calcium in a muscle cell collected from an animal which has been received a treatment with a substance or factor to be tested; and (b) a step of identifying the tested substance or factor as a candidate for a substance or factor capable of promoting muscle hypertrophy on the basis of the results obtained in step (a).
CA2396734C Extraction of flavonoids A method of producing an enriched flavonoid aglycone extract from starting material containing a suitable flavonoid glycoside and/or conjugate thereof comprising the steps of: (i) enzymatically converting the flavonoid glycoside or conjugate thereof into the flavonoid aglycone; (ii) adjusting the pH to render the flavonoid aglycone soluble and removing the insoluble fraction; and (iii) adjusting the pH to render the soluble flavonoid aglycone relatively insoluble and forming an extract containing the same.
WO2012044537A1 Substituted benzimidazole and imidazopyridine compounds useful as cyp17 modulators Disclosed are heteroaryl compounds of Formula (I), (I), or pharmaceutically acceptable salts thereof, wherein Z is CH or N; W is CR3 or N; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
CN101235061B Novel alpha-amylase inhibitor alcaftadine series compounds and application thereof A new quasi-oligosaccharide alpha-amylase inhibitor as alcaftadine compounds has a structure of formula (I) as the follows: wherein m is integer as 0 to 7, n is integer as 1 to 4 and q is integer as 0 to 3, The mixture and monomer of the alcaftadine compound are white amorphous powder which dissolves in water and DMSO easily, dissolves in methanol, alcohol and acetone slightly and not dissolves in other organic solvents. The alcaftadine compound contains different amounts of acarviosine-amylaceum structural units and reducing glucose terminals, especially the compound with high repeated times has a structure significant different from the prior quasi-oligosaccharide alpha-amylase inhibitor. Therefore, the compound is a new quasi-oligosaccharide alpha-amylase inhibitor with the application for preparing the drug of diabetes and adiposis or the like.
CN1844084A Beta-elemene amino acid or carboxylic acid derivatives and preparation process and use thereof The invention discloses a A-elemene amino acid or carboxylic acid derivants, Process for preparing, usage and preparation; the structural formula of derivant is III. Wherein R represent C2-C20 every kinds of alpha-, beta-, gamma- amino acids; Every kinds of amino acids of C1-C20; wherein cyclohexane skeleton has three chirality center. This derivant is used to improve water-solubility and anticancer active of A-elemene amino acid, introducing amino acid which contains synthetic compounds of amidol or carboxy group, this derivant has stronger physiologically active and larger polarity, reaching the purpose of improving water-solubility.
US20120225849 2-Methoxyestradiol (2-ME2) Prodrug with Enhanced Bioavailability for Prophylaxis or Treatment of Cancerous or Non-Cancerous Condition A prodrug of 2-methoxyestradiol (2-ME2) can be used for prophylaxis or treatment of cancer, such as esophageal cancer, prostate cancer, or breast cancer, and/or a non-cancerous condition, such as rheumatoid arthritis or pre-clampsia.
CN101896501A Antibody targeting osteoclast-related protein Siglec-15 The invention provides a method of detecting an abnormality in bone metabolism by using a gene strongly expressing in osteoclasts; a method of screening a compound having an effect of treating and/or preventing an abnormality in bone metabolism; and a medicinal composition for treating and/or preventing an abnormality in bone metabolism. A method of detecting an abnormality in bone metabolism by using the expression of human Siglec-15 gene as an indication; a medicinal composition containing an antibody which has an activity of specifically recognizing human Siglec-15 and inhibiting the formation of osteoclasts; and so on.
CN103159769A Doxofylline compound and medicine composition thereof The invention relates to a doxofylline crystal compound. Determined by adopting X-ray powder diffraction, the doxofylline crystal compound has he characteristic peak at 2theta+/-0.2 degrees of 11.8 degrees, 13.3 degrees, 16.8 degrees, 19.2 degrees, 20.8 degrees, 23.3 degrees, 26.3 degrees, 26.7 degrees, 28.2 degrees, 29.9 degrees, 31.3 degrees, 32.7 degrees, 36.8 degrees and 41.1 degrees. The invention also relates to a preparation and a medicine composition preparation containing the doxofylline compound, wherein the medicine composition preparation is freeze-dried powder, injection, tablets and capsules. The doxofylline freeze-dried powder, injection, tablets and capsules which are provided by the invention are simple in formulation and technology, have obviously improved stability and improve the safety and effectiveness of medicine using.
US7320875 Screening for neutralizing hepatitis C virus antibodies in a blood sample utilizing an HCV E2 protein and a protein from a human or chimpanzee cell that has a molecular weight of 24 kd that binds to the E2 protein of HCV; comparing the amount of bound proteins to that in the absence of HCV antibodies HCV assays are described. The assays utilize a 24 kd protein capable of binding the E2 envelope protein of hepatitis C virus (HCV), or functionally equivalent variants or fragments of the 24 kd protein.
US7709539 has been shown to have free radical scavenging, anti-inflammatory and anti-thrombogenic activities in biological systems; resveratrol has also been shown to be a good cancer preventive chemical and has been recommended as a food supplement for health benefits; can effectively lower blood sugar Resveratrol, an antioxidant found in various fruits, vegetables, grapes, and red wines, has been shown to have free radical scavenging, anti-inflammatory and anti-thrombogenic activities in biological systems. Moreover, resveratrol has also been shown to be a good cancer preventive chemical and has been recommended as a food supplement for health benefits. Resveratrol can effectively lower the blood sugar in both type 1 (insulin-dependent diabetes mellitus, IDDM) and type 2 (insulin-independent diabetes mellitus, NIDDM) diabetic rats. Resveratrol could also delay the onset of the insulin-resistant phenotype in experimental rats with prolonged injection of insulin. Further, resveratrol simultaneously slows down the body weight increment compared with untreated insulin resistant animals.
CN102068455A Prescription for treating red skin disease The invention discloses a prescription for treating a red skin disease. The treating prescription comprises the following components of: sodium chloride, potassium permanganate, streptomycin sulfate, diatomite, chitin and water. The prescription for treating the red skin disease has ideal curative effects on the red skin disease, and the main components of the prescription are natural materials without toxicity or side effects. the prescription has the characteristics of good biocompatibility, stable and durable curative effects, wide raw material source and low cost.
CA2794503A1 Aerosol foams comprising clindamycin phosphate Described herein are emulsions and compositions for the treatment of acne vulgaris. The emulsions may be formulated as aerosol compositions. The aerosol propellant may be a hydrofluoroalkane propellant. The emulsions or compositions may comprise clindamycin phosphate and a buffer salt, and may exhibit decreased rates of clindamycin phosphate hydrolysis. Also described are methods of treating acne vulgaris, comprising the step of applying to an affected area of a subject in need thereof a therapeutically-effective amount of an inventive emulsion or aerosol composition.
CN101336895B Novel alkalized solid-liquid two-state skin quick-anaesthesia nano-emulsion and preparation method thereof The invention relates to a novel alkalized liquid-state and solid-state rapid skin anesthesia nanometer emulsion for skin external application and a preparation method thereof. The inventive nanometer emulsion mainly comprises three systems: the first system is a skin anesthesia effective ingredient system, the second system is a nanometer emulsion composition system, and the third system is a nanometer emulsion excipient protective system. The three systems can be used for preparing a liquid-state and solid-state rapid anesthesia nanometer emulsion for skin external anesthesia. The inventivenanometer emulsion compounds three anesthetics with respective characteristics and contains menthol, so that the formula is more reasonable and the effect is more distinct, wherein tetracaine has strong transdermal capacity, rapid action and strong local anesthetic action, the anesthetic action of chloroprocaine is 4-6 times stronger than procaine and 2-3 times stronger than lidocaine, and the chloroprocaine has low toxicity, high penetration capacity, quick action and long-lasting anesthetic action.
CN102958523A Antitumor agent using compounds having kinase inhibitory effect in combination Disclosed is an antitumor agent which uses a compound represented by formula (I) or a pharmacologically acceptable salt thereof in combination with a compound represented by formula (II) or a pharmacologically acceptable salt thereof. The antitumor agent exhibits remarkable antitumor effect in comparison to the cases where each one of the above-mentioned compounds is used alone. In addition, the antitumor agent exhibits antitumor effect on various kinds of cancer. (In the formulae, R1 represents an azetidinyl group or the like; R2 to R5 each represents a hydrogen atom or a halogen atom; R6 represents a C3-8 cycloalkyl group or the like; R7 represents a hydrogen atom or the like; and R8 represents a halogen atom or the like.)
CN1732924A Andrograpolide sodium bisulphite injection and preparation process thereof The invention relates to andrograpolide sodium bisulphite injection and preparation process, wherein the injection comprises sodium bisulphate, andrographolide 0.2-12.55, auxiliary materials 0-25.0%, cushioning modifier or stabilizator 0.005-1.0%, and water for injection.
CN103301102A Method for extracting antioxidant from myricaria laxiflora and application thereof The invention relates to an extraction method of an antioxidant and an application in protection of nerve cells against oxidation by utilizing the antioxidant, belonging to the technical field of biological medicines. The extraction method disclosed by the invention comprises the following steps of: taking myricaria laxiflora as a raw material, taking ethanol as an extraction solvent, performing Soxhlet extraction, performing cold leaching on a crude extraction solution with HCl, adjusting the pH with saturated NaCO3, extracting with chloroform, performing chloroform-methanol gradient elution by silica gel column chromatography, performing Sephadex LH-20 gel column methanol elution, and further performing crystallization and re-crystallization to obtain the antioxidant. The antioxidant is identified as 3, 4-dimethoxy-5-methylparaben by 1H-NMR and 13C-NMR, the molecular formula is C10H12O5, and the anti-oxidation property and the free radical scavenging activity are stronger. The concentration of the antioxidant is 0.5-12.5mu g/mL, when the dosage is 100mu L, the toxicity of the natural antioxidant against SH-SY5Y cells is less than 3.4%, the relative survival rate against human neuroblastoma cells SH-SY5Y after oxidative damages by hydrogen peroxide is 50-80%, and the antioxidant has a better anti-oxidation protection effect in comparison with PG (propyl gallate), can be used as a natural non-toxic antioxidant and can be applied to the fields of foods, medicines, cosmetics and the like.
US20120172453 Methods for treating neurodegenerative diseases This invention relates to the 5-cis and 5-trans isomers of geranylgeranyl acetone, preferably such synthetic isomers, and pharmaceutical compositions containing such isomers. Other aspects of this invention relate to the use of geranylgeranyl acetone and its isomers in methods for inhibiting neural death, increasing neural activity, and increasing axon growth and cell viability. Geranylgeranyl acetone is a known anti-ulcer drug used commercially and in clinical situations. GGA has also been shown to exert cytoprotective effects on a variety of organs, such as the eye, brain, and heart.
CA2348395C Compositions comprising a mixture of bioflavonols The present invention relates to novel compositions containing a mixture of two or three bioflavonols like isoquercetin, quercetin-4'-glycoside, rutin and quercetin, which show differences in their pharmacokinetics. These compositions are useful as food supplements possessing preventive properties against damage to human tissues due to their antioxidant properties. Furthermore, these compositions secure a continuum of the presence of bioflavonols having the same aglycone in human plasma over an extended period of time.
CN101214253A Application of anemarrhenasaponin B-II in preparing antidepressant product The present invention relates to a novel purpose of timosaponin B-II. The anti-depression test of the timosaponin B-II in total timosaponin extract shows obvious anti-depression activity; The present invention has strong pharmacological effect and stable quality; the raw material of the present invention has abundant source, cheap price and is safe with low toxin; the present invention has simple preparation technology and high yield, which provides a novel medicine source for preventing, diagnosing, examining, protecting, remedying and researching on the depression and diseases directly related to the depression, is fit for the industrialization production, is easy for popularizing, applying and has very important value for developing and using Chinese officinal plant resource. Affective mental disorder is listed at top in Chinese disease general burden, and the research and manufacture of the drug for preventing and remedying the depression has obvious social benefit and economic benefit.
CN1562996A Extract products of exopleura of sorghum, extracting method and application This invention process consists of procedures of: raw material kaoliang external seed husk is crushed, sieve extracted, vacuum distillation concetrated, filtered, impurity removed; then, extracted, concentrated, added with crystallization agent to separate precipitate. Then it is proceeded with another purification step, to obtain extract of external seed husk of kaoliang with high anti-oxidation function. advantages are: low cost of raw material, simple prodn. process, low pollution, comerciazation prodn., its waste can be used as fodder, the product is used as health-care food benifit to liver.
CN103442704A Cystamine analogues for the treatment of parkinson's disease The present invention relates to the use of cystamine analogues for the treatment of Parkinson's disease. The present invention also relates to the use of composition comprising cystamine analogues and cysteine. The present invention relates to a method for modifying the progression of Parkinson's disease comprising administering a therapeutically effective amount of at least one cystamine analogue or a pharmaceutically acceptable salt of a cystamine analogue to a patient in need thereof.
WO2014026121A1 Methods and compositions for treating conditions related to lack of blood supply, shock and neuronal injuries A pharmaceutical composition comprising an amphiphilic emulsifier, a polar liquid carrier and, optionally, a lipid component. The amphiphilic emulsifier form free-moving, optionally lipid-carrying, micelles (LMs) in the polar liquid carrier. The pharmaceutical composition is free of hemoglobin and fluorocarbon and can be used for treating conditions related to lack of blood supply and to raise the blood pressure and correct hypovolemia.
US20130158108 Uses of n-butylidenephthalide in treating a liver injury and improving liver function Provided is a method for treating a liver injury such as fibrosis, cirrhosis and hepatitis as well as a method for restoring liver function in a subject, which includes administrating to the subject a therapeutically effective amount of n-butylidenephthalide having the formula (I) as an active ingredient, or a pharmaceutically acceptable salt of ester thereof: wherein R is ═CHCH2CH2CH3, and n-butylidenephthalide (I) is E form, Z form or a mixture thereof.
CN101142182B Method of preparation of pure 4-pyrrolidinophenylbenzyl ether derivatives as MAOB inhibitors The invention relates to a method for preparing enantiomerically pure 4- pyrrolidinophenylbenzyl ether derivatives of formula I wherein R<1>, R<21>, R<22>, R<23>, R<24> and n are as defined in the description and claims and to intermediates useful in the method of the invention as well as salts thereof.
CN102895360A Medicine for treating dental ulcer The invention relates to a medicine for treating a dental ulcer. The medicine for treating the dental ulcer is prepared from the following raw materials in parts by weight: 10-20 parts of jasmine, 15-30 parts of borneol, 5-10 parts of alum, 2-8 parts of cinnabar, 1-3 parts of honeysuckle and 1-4 parts of Coptis chinensis, wherein the jasmine has the functions of clearing heat-fire; the borneol has the functions of clearing away heat and toxic materials and preventing rot to promote tissue regeneration; the cinnabar has the function of inhibiting or killing skin bacteria and parasites; the honeysuckle is sweet and cold in nature and is fragrant; the sweet and the cold are capable of clearing heat without hurting the stomach; the fragrance penetrates and is capable of eliminate evil; the honeysuckle not only is capable of dispelling wind-heat but also is capable of removing summer-heat and blood toxin; and the Coptis chinensis has the functions of clearing heat and drying dampness and purging fire for removing toxin. According to numerous experiments and summaries, the formula for treating the dental ulcer is good in clinical experiment result and high in efficiency, and the cure rate reaches 80-95 percent at a time.
CN101569618B Application of long-chain fatty acid derivative or plant extracts containing same in inhibiting the activity of aromatizing enzyme The present invention discloses an application of a long-chain fatty acid derivative shown as formula 5 or plant extracts containing the same in preparing preparations to inhibit the activity of aromatizing enzyme and in preparing pharmaceutical compositions to prevent or treat prostatoplasia diseases. The application opens up a new application field for the compound and also provides a new way for preventing and treating the diseases in the field. In the formula 5, B is N-(2-ethoxyl), sorbitol group, fructosyl or H; A is (CH2CH=CH)3.
CN101401817A Preparation for pharmaceutical chemicals for solubilizing uropoiesis stone The invention provides a method for preparing a chemical drug dissolving a urinary stone. The urinary system stone in human body comprises a kidney stone, a ureter stone, a vesical stone and a urethral stone. The main means of treating the urinary stone adopt a crusher and an operation, but the means can not meet social needs because of a plurality of contraindications and high after-operation recurrence rate, so that in the society, a medical drug dissolving the stone is urgently needed. However, so far, no drug dissolving the stone has been found and used. The preparation method comprises the following: the invention is a compound; and potassium nitrate and aluminum potassium sulfate containing crystal water are mixed according to the weight ratio of 1 to 1, ground, encapsulated and is taken by a patient. The taking method is as follows: under general conditions, 6 to 10 capsules with about between 5 and 10 grams are taken for each day; for a patient with severe hydronephrosis, about 15 capsules are taken for each day; when the hydronephrosis is discharged, the dose is reduced; the capsules are taken after dinner, and taken for multiple times as possible, and 2 to 3 capsules for each time properly; moreover, the patient needs to drink more water; after curing, for preventing the urinary stone, one capsule is taken for each day, so that people in high occurrence areas and ages can take the capsules for early prevention.
WO2008128045A1 Solid forms of (e) -1- (4- ( (1r, 2s, 3r) -1, 2, 3, 4-tetrahydroxybutyl) -1h-imidazol-2-yl)ethanone oxime Amorphous and crystalline solid forms of (E)-1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone oxime are disclosed. These specific solid forms may be used as sphingosite-1 phosphate modulators for treating autoimmune and inflammatory diseases.
WO2008093655A1 Polyalcohol compound and pharmaceutical agent Disclosed is a polyalcohol compound which is highly water-soluble, can be formulated into a preparation readily, can be reduced in its dose amount, and can be used as an active ingredient for an antihyperlipidemic agent. The polyalcohol compound is represented by the formula (I). (I) wherein R represents a residue produced by removing a carboxyl group or an ester group from a fibrate-type antihyperlipidemic compound; X represents a linkage group for linking n pieces of polyalcohol moieties to R; and n represents an integer of 1 to 8.
US20050255126 biologically pure strain of Aureobasidium pullulans isolated from a food source; culturing in a medium containing saccharides as a carbon source; has resistance to the antibiotic cycloheximide A β-glucan-containing fat and oil composition contains β-glucan of microorganism origin or basidiomycete origin. The β-glucan-containing fat and oil composition has β-glucan uniformly dispersed in a food without worsening the texture, taste etc. of the food. The novel microorganism can efficiently produce β-glucan which has a high activity and favorable qualities as β-glucan of microorganism origin as described above from less expensive saccharides such as sucrose at a high production speed.
EP2533777A1 Pharmaceutical compositions comprising fluticasone, tiotropium and sodium cromoglycate A pharmaceutical composition comprising tiotropium bromide with water content less than or equal to 2.5%, fluticasone propionate and sodium cromoglycate, and its use in the symptomatic and/or prophylactic treatment of respiratory diseases, especially in asthma, allergic rhinitis, chronic obstructive pulmonary disease (COPD).
US20110189288 Diethylstilbestrol dosage form and methods of treatment Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, particularly diethylstilbestrol and pharmaceutically acceptable salts thereof to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.
WO2013180240A1 Medicine comprising combination of general anesthetic drug and hydrogen The purpose of the present invention is to provide a general anesthetic medicine which can prevent and/or alleviate an anesthetic-induced neuropathy in the brain (preferably the developing brain). The present invention relates to a medicine which can prevent and/or alleviate an anesthetic-induced neuropathy in the brain (preferably the developing brain), said medicine comprising a combination of a general anesthetic drug and hydrogen.
CN101423508B Method for preparing flavonoid from lotus leaf and drug application thereof The invention provides a method for preparing lotus leaf flavone and medicinal application thereof. The method comprises the following steps: crudely extracting and concentrating the lotus leaf flavone; performing chromatography on the extract by polyamide chromatography column; carrying out gradient elution by water and ethanol; collecting the part eluted by the ethanol of between 50 and 90 percent; concentrating the part until drying the part under decompression condition; and dissolving the dried part by distilled water. The flavone prepared by the method and added to medicinal carrier and/or pharmaceutically accepted adjuvants can be used as injection, tablets, pills, capsules, troches, suspending agents, emulsion, suppositories or aerosols. The flavone has the function of activating the activity of glucokinase, and can be used for preventing and treating diseases mediated by the glucokinase.
WO2012155981A1 New process for the synthesis of rifaximin and a new pseudo-crystalline form of rifaximin obtained thereby Process for the preparation of rifaximin, pseudo-crystalline rifaximin and a new pseudo-crystalline form of rifaximin with fewer impurities obtained thereby.
CA2446221C Stable powder inhalation dosage formulation An insufflation for the administration of a drug into a body cavity is described where the carrier for the drug is a finely divided powder selected from the group consisting of myoinositol,mannitol and cellobiose.
US20080226640 Mixture comprising serum complement system protein (INSP162) use in preparation of vaccines and antibodies for treatment and prevention of infcetion, cell proliferative, skin, neurodegenerative, bone, inflammatory, respiratory system and autoimmune disorders This invention relates to a novel protein, termed INSP162, herein identified as a secreted protein containing c1q and collagen domains and to the use of this protein and nucleic acid sequence from the encoding gene in the diagnosis, prevention and treatment of disease.
US7531527 (20R)-1 alpha ,25-dihydroxy-2-[3'-hydroxypropylidene]-19-norvitamin D3; high intestinal calcium transport activity; ability to mobilize calcium from bone; bone replacement surgeries, autoimmune diseases, multiple sclerosis, diabetes mellitus,lupus, antiproliferative agents 2-propylidene-19-nor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by high bone calcium mobilization activity and high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis, as well as autoimmune diseases such as multiple sclerosis, diabetes mellitus and lupus. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis. These compounds also increase both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.
WO2007008672A1 Crystalline cefdinir trihemihydrate A novel crystalline cefdinir trihemihydrate , ways to make it and use it, compositions comprising it and made with it, and methods of treatment using it are disclosed.
WO2007053095A1 Chroman compounds as 5-ht1b antagonists Chroman derivatives according to formula (I), wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same. The compounds are 5-HT1B antagonists and are useful in the treatment of mood and anxiety disorders .as well as cognitive disorders.
WO2008038302A2 Therapeutic formulation comprising a sulfonylurea, metformin and a nitric oxide scavenger. A therapeutic formulation comprising of Sulfonylureas as active agents namely, Glibenclamide, Gliclazide, Glimepiride, Glipizide and Gliquidone, characterized in that said Sulfonylureas are combined with Metformin and combined or complexated with NO Scavenger to prevent Diabetic Complications arising out of Nitrosative stress.
WO2010081257A1 Composition comprising bacillus calmette guerin polysaccharides and bacillus calmette guerin nucleic acids and use of preparing medicament thereof A composition comprising Bacillus Calmette Guerin polysaccharides and Bacillus Calmette Guerin nucleic acids is provided, wherein said polysaccharides are comprising 10%-69% by mass of the composition and said nucleic acids are comprising 30%-89% by mass of the composition. The composition is made by mixing said polysaccharides and said nucleic acids, wherein said polysaccharides and said nucleic acids are obtained from the Bacillus Calmette Guerin cultures by the following process: extracting the mixture of said polysaccharides and said nucleic acids from said Bacillus Calmette Guerin cultures, and separating said polysaccharides and said nucleic acids from the mixture by ion exchange chromatography. The use of the composition comprising said polysaccharides and said nucleic acids for preparation of a biological medicament for treatment or prevention of microorganism infections, tumors, allergic reactions and the like is also provided.
WO2014113406A1 Compositions and methods for treating pancreatic cancer The present disclosure provides compositions and methods for treating or reducing the risk of pancreatic cancer by administering compounds capable of inhibiting the expression or activity of RUNX3.
CN102068407B Cabazitaxel injection and preparation method thereof The present invention provides cabazitaxel injection. The injection of each milliliter comprises the following components by weight: 10 to 100 milligrams of cabazitaxel, 250 to 800 milligrams of polysorbate 80, 200 to 600 milligrams of absolute ethanol, and 0.05 to 20 milligrams of citric acid. The cabazitaxel injection is a single preparation, does not need to be previously dissolved and prepared by using a special solvent, and can be directly diluted for administration; compared with the conventional preparation technology, the preparation has simple preparation process, low cost and good stability; meanwhile, the preparation shortens the time for preparing the medicinal liquor, improves the stability of clinical medicinal liquor, enhances the accuracy of administration dose, and reduces toxic or side reaction; and the preparation simplifies the preparation process of medicinal personnel, and reduces the risks of the preparation process on harm to the medicinal personnel and environmental pollution.
US20080175909 Delivery device containing venlafaxine and memantine and method of use thereof The present invention provides an osmotic device containing controlled release venlafaxine in the core in combination with an anti-Alzheimer's or an anti-Parkinson's drug in a rapid release external coat. Memantine is used as an anti-Alzheimer's drug or an anti-Parkinson's drug. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray-coated rather than compression-coated onto the device. The device is useful for the treatment of symptoms associate with Alzheimer's disease and/or Parkinson's disease patients. The device and method can also be used to treat or ameliorate other symptoms associated with Alzheimer's disease, Parkinson's disease or any other neurological disorder. Other dosage forms that provide a controlled, sustained or extended release of venlafaxine in combination with a rapid or immediate release of memantine are useful in the invention.
US20110183915 Small Molecule Cancer Treatments that cause Necrosis in Cancer Cells but do not Affect Normal Cells A method of treating cancer in a subject, including: providing a subject having a plurality of cancer cells; and administering to the subject, a therapeutically effective amount of a composition including: an HDM-2 binding component; and a membrane resident component, the membrane resident component bound to the HDM-2 binding component. Also provided are a method of selectively necrosing cancer cells, a method of causing membranolysis in cancer cells, and a cancer treatment composition.
US20100152286 Method for Producing Fucoxanthin The present invention provides a method for producing fucoxanthin extract, said method comprising: performing absorption of the fucoxanthin extract by using absorbent and then performing elution to remove heavy metals and arsenic salt contained in the fucoxanthin extract, wherein the absorbent is selected from a group having macroporous resin, polyamide, activated carbon, alumina and a combination thereof. The method for producing fucoxanthin extract according to the present invention, the content of heave metal in the fucoxanthin extract can be reduced, while the content of fucoxanthin in the fucoxanthin extract can increase. In addition, the present invention also provides a fucoxanthin extract obtained by the above method, as well as fucoxanthin products containing the fucoxanthin extract.
CN101200460A Dihydrobenzopyrans ketone compound and uses thereof The invention relates to the new synthesized compound i.e. dihydrobenzo pyrone type and the application thereof, and belongs to the field of the chemical drug. The experiment results shows that the compound (I) can kill the breast cancer cell MCF7 expressing ER Alpha 66, FR Alpha 46 and ER Alpha 36. Moreover, the compound (I) can be served as the regulator of the estrogen receptor ER Alpha 36 for treatment of the illness caused by the unusual expression of the estrogen receptor ER Alpha 36, such as the tumor, the osteoporosis, the asthma, the heart disease and the senile dementia, etc.
WO2012016980A2 Use of sigma ligands in opioid-induced hyperalgesia The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat opioid-induced hyperalgesia (OIH) associated to opioid therapy.
CN103228631A Kat II inhibitors The present invention relates to compounds 3-amino-1-hydroxy-2-oxo-1,2,3,4-tetrahydroquinoline-7-carbonitrile, 3-amino-1-hydroxy-7-(2-methoxyethoxy)-3,4-dihydroquinolin-2(1H)-one, and 3-amino-1-hydroxy-7-[(1S)-2-methoxy-1-methylethoxy]-3,4-dihydroquinolin-2(1H)-one, including racemic mixtures and resolved enantiomers thereof, to pharmaceutically acceptable salts thereof, and to the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
WO2005105097A3 Pyridopyrimidines for treating inflammatory and other diseases The present invention relates to the use of pyridopyrimidine derivatives having the general formula (I) wherein X represents =NH, =N-Acyl, =O, or =S; R1 represents -NR3R4, -SR3, -SO-R3, -SO2-R3, -OR3; R2, R3, and R4 are independently of each other hydrogen, -(CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR5R6, phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R5 and R6 are independently of each other hydrogen, (CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; R5 and R6 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ph* represents phenyl or substituted phenyl; n is 0, 1, 2, or 3; R4 can optionally be -CO-R3, -CO-OR3, -SO2-R3, -SO2-NR5R6, -CO-NR5R6, -CS-NR5R6, -C(=NH)-R3, -C(=NH)-NR5R6; R3 and R4 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ar represents phenyl, substituted phenyl, or heteroaryl; and pharmaceutically acceptable salts thereof for prophylaxis and/or treatment of inflammatory diseases, neurodegenerative disorders, immunological diseases, neuroimmunological diseases, autoimmune diseases, diabetes, transplant rejection, infective diseases, prion diseases, cardiovascular diseases and disorders.
US20070014857 Pharmaceutical formulation having a masked taste and method for the production thereof The invention relates to a pharmaceutical formulation in the form of a powder which is administered orally in an aqueous suspension, having a masked taste, and comprising at least one cellulose polymer, a methacrylic polymer and an active ingredient which is distributed in a homogeneous manner in a molecular state in an atomized matrix, in addition to an alkaline agent and an adsorbing agent, a method for the production thereof and a method for masking the taste of pharmaceutical products.
EP1108026B1 Nucleic acids encoding ataxin-2 binding proteins, products related thereto and methods of using same In accordance with the present invention, there are provided novel isolated nucleic acids encoding ataxin-2-binding proteins (A2BPs), functional fragments thereof, vectors containing invention nucleic acids and recombinant cells transformed therewith, antisense-nucleic acids thereto. Also provided are novel isolated ataxin-2-binding proteins (A2BPs) having ability to bind to ataxin-2, methods for expression of A2BP, transgenic non-human mammals that express invention A2BP, anti-A2BP antibodies, and methods related thereto.
CN102603743A Anti-tumor benzazepine[f]azulene derivative, preparation method thereof, and purpose thereof The invention relates to the field of pharmaceutical chemistry, and specifically relates to a benzazepine[f]azulene derivative (I) and an anti-tumor function thereof. As a result of pharmacological tests, the compound provided by the invention has in-vivo and in-vitro anti-tumor activities, and can be used to be developed into clinical medicines used for treating or controlling diseases such as stomach cancer, lung cancer, liver cancer, breast cancer, colorectal cancer, prostate cancer, and mouth cancer.
WO2006128462A1 Sertindole titration The present invention relates to methods for administering sertindole to schizophrenic patients. More specifically, the present invention relates to monitoring the ECGs of patients receiving maintenance dose sertindole therapy for the presence of QTc interval prolongation or torsade de pointes.
CN103183623A A group of benzene sulfonamido benzamide derivatives, and preparation and application thereof The invention relates to a group of benzene sulfonamido benzamide derivatives, and a preparation method and an application thereof. The research results indicate that the compounds obviously inhibit the apical sodium-dependent bile acid transporter (ASBT) at the cellular level, thereby being expected to be researched and developed to become a clinically effective medicament for treating hyperlipemia and cholestatic diseases.
US20080275109 Drug, food or drink product containing proanthocyanidine derived from hop, hop bract or apple; prevents digestive diseases caused by Helicobacter pylori; freeze drying A drug, quasi drug, food or drink product containing a proanthocyanidine derived from hop, hop bract or apple has the effect of neutralizing or attenuating a vacuolacting toxin produced by Helicobacter pylori, thus preventing, preventing recurrence or treating digestive diseases in which Helicobacter pylori participates, as well as killing Helicobacter pylori, while providing few side effects and being free of risk of the occurrence of a tolerant strain.
CN102030811A Phytolaccagenin derivative and preparation method and application thereof The invention discloses a phytolaccagenin derivative and a preparation method and application thereof. The general formula of the derivative is shown in the specifications, wherein R is amino acid, polypeptide, piperazinyl, substituted piperazinyl or substituted amidogen. An active ester intermediate which is formed by phytolaccagenin under the action of a condensing agent reacts with amine or piperazine or N-substituted piperazine or protected amino acid of carboxyl or polypeptide, and the reaction product is separated and purified so as to obtain the phytolaccagenin derivative. The phytolaccagenin derivative, pharmaceutic salt and a medicinal composition of the phytolaccagenin derivative can be used for preparing an anti-inflammatory medicament.
US20120189711 Modular Extracorporeal Systems and Methods for Treating Blood-Borne Diseases Extracorporeal systems and methods for treating blood-borne diseases in a subject or for developing drugs to treat blood-borne diseases include various environmental and treatment modules that can be tailored to a specific disease or infection. In certain embodiments of the systems and methods, a blood sample is treated with hydrostatic pressure, a pulsed electrical field, a pharmaceutical agent, microwave, centrifugation, sonification, radiation, or a combination thereof, under environmental conditions that are effective for the treatment.
CN101579324B Method for preparing omeprazole enteric fast-release tablet The invention relates to the field of pharmaceutical preparations, in particular to a method for preparing an omeprazole enteric fast-release tablet, which is characterized in that in the preparing process with a conventional method, omeprazole is dispersed in binding agent suspension solution, the mixture is granulated by a fluidized bed through top spraying, and the grain size is between 80 and120 meshes. Besides, a sealing coat of the omeprazole enteric fast-release tablet comprises a first sealing coat and a second sealing coat, wherein the first sealing coat contains hydroxypropyl methylcellulose and a basifier, and the second sealing coat contains the hydroxypropyl methylcellulose, smoothers and titanium dioxide. An in vitro dissolution experiment shows that the omeprazole enteric fast-release preparation prepared by the method is dissolved for 100 percent at the 15th minute; and an acid resistance test shows that a coating tablet has no obvious change in two hours in an environment of which the pH is 1.2.
WO2006135083A1 Prophylactic or therapeutic agent for visceral fat syndrome Disclosed are a pharmaceutical for the prevention or treatment of visceral fat syndrome and a beverage/food for the prevention or amelioration of the disease. A prophylactic or therapeutic agent for visceral fat syndrome comprising luteolin and/or a glucoside thereof; a commercial package comprising the prophylactic or therapeutic agent and a sheet of paper having thereon the words 'this prophylactic or therapeutic agent can be used or is recommended to be used for the prevention or treatment of visceral fat syndrome'; and a beverage/food for the prevention or amelioration of visceral fat syndrome comprising luteolin and/or a glucoside thereof, preferably the food/beverage having a label on which the words 'this product is intended to be used for the prevention or amelioration of the disease' are described.
US20120220622 Heterocyclic derivatives The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
WO2011014515A1 2, 7 -naphthyridin- 1 -one derivatives as syk kinase inhibitors Provided herein area novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.
US20080275055 4-(4-methyl-piperazin-1-ylmethyl-benzoic acid with N-(5- amino-2-methylphenyl)-4-(3pyridyl)-2-pyrimidine-amine in the presence of a coupling reagent such as 2-(5-norborene-2,3- dicarboximido)- 1,1,3,3-tetramethyluronium tetrafluoroborate to produce imatinib, salt formation wtih methanesululfonic acid Provided is a process for producing imatinib and salts thereof, e.g., imatinib mesylate. The process includes reacting4-(4-methyl-piperazin-1-ylmethyl)-benzoic acid with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidine-amine in the presence of a carboxylic acid coupling reagent, to produce imatinib, and optionally converting the imatinib into a salt.
CN102212091A High-purity geniposide as well as preparation and clinical application of preparations thereof The invention provides high-purity geniposide as well as preparation and clinical application of preparations thereof. Gardenia is a dried and matured fruit of rubiaceae plant gardenia and has liver-protecting, chole-promoting, pressure-reducing, heat-clearing, cold-promoting and diarrhea-relieving functions and the like. The geniposide is a product which is obtained by refining the dried and matured fruit of the rubiaceae plant gardenia by virtue of a high-technology production process and is an iridoid glycoside compound. The geniposide is used for treating cardiovascular and cerebrovascular diseases, hepatic and biliary diseases, diabetes mellitus and the like. At present, a lot of methods for extracting the geniposide and gardenia pigment from the gardenia are reported in documents, but a plenty of problems exit, such as the product contains high impurity content so that the requirements of customers at home and abroad can not be satisfied, the production cost is high, the yield is low, the economic benefits are poor, the methods are not suitable for industrial production, and the like. According to the invention, the problems are solved. The high-purity geniposide is obtained by virtue of extraction and purification of gardenia and is prepared into proper preparations such as tablets, capsules, particles, injecta, powder injections, infusion solutions and the like to be applied to the clinic for treating cardiovascular and cerebrovascular diseases, hepatic and biliary diseases, diabetes mellitus and the like.
US20100028468 Formulations containing thymoquinone for urinary health A novel dietary supplement or therapeutic composition is provided that serves to treat lower urinary tract disorders or to support normal urinary tract function in animals. The supplement comprises a thymoquinone formulation and at least one member of the group consisting of cranberry fruit, cranberry extract, cranberry juice and a pharmaceutical grade methionine.
CN101125201A Medicine composition for treating osteoporosis or preventing bone fracture caused by osteoporosis and its application The present invention provides a pharmaceutical composition containing alendronate or the pharmaceutical acceptable salt thereof and parathyroid hormone or the derivatives thereof, the pharmaceutical composition can also be added with vitamin D and calcium salt. The pharmaceutical composition of the present invention can be used for the treatment of osteoporosis, on the one hand, the present invention can inhibit the bone resorption fundamentally, on the other hand, the present invention can increase the bone mass and improve the bone formation, the two-pronged approach can ensure the patients to get the scientific and comprehensive treatment, so as to achieve the purposes of treatment of osteoporosis, the prevention of occurrence of bone fracture and the treatment of the fractures caused by osteoporosis.
EP2005948A9 Perfluorocarbon gas transferring emulsion for medico-biological use, the composition and the production method thereof a medicinal agent The invention belongs to medicobiological industry and refers to the composition, method of production and use of the means, based on perfluorocarbon emulsions, intended as the blood substitute means and other remedies. The essence of invention consists in creation of method and composition made from the mixture of two perfluorocarbons: fast eliminated (Sv-syu) and (or) slowly eliminated (Sc-sp), as perfluorodecaline (PFD) / perfluoromethyl-cyclo-hexylpiperidine (PFMCP), or PFD/perfluorotributylamine (PFTBA), or perfluorooctylbromide (PFOB)/PFMCP, or PFOB/PFTBA, or PFOB/PFD, or PFMCP/PFTBA in ratio from 1/1 to 10/10, respectively; or a mixture of three perfluorocarbons: two are fast eliminated (C8-C10) and one is slowly eliminated (C11-C12), or of one fast eliminated (C8-C10) and two slowly eliminated (C11-C12), as PFOB/PFD/PFMCP, or PFOB/PFD/PFTBA, or PFOB/PFMCT/PFTBA, or PFD/PFMCP/PFTBA in ratio from 1/1/1 to 10/10/10, respectively; or a mixture of four perfluorocarbons: two of them are fast eliminated (C8-C10) and two slowly eliminated (C11-C12) PFOB/PFD/PFMCP/PFTBA in ratio from 1/1/1/1 to 10/10/10/10, respectively; a mixture of perfluorocarbons in emulsion from 1% (0,5 vol.%) to 100% (50 vol. %) with average particle size 30-80 nm, is emulsified by proxanol-268 from 0,2% to 20% with molecular weight 6-12 thousand Da, has acceptable electrolytic solution.
WO2010133087A1 Compositions and methods for treating inflammatory arthritis Methods for treating or preventing one or more symptoms of rheumatoid arthritis or other types of inflammatory arthritis involves administering a composition containing an effective amount of arsenic trioxide to an affected patient. The composition comprising arsenic trioxide can be administered orally, for example, as a solution, suspension, syrup, emulsion, tablet, or capsule.
CN103027891A Acetylcysteine gargle for treating dental ulcers, and preparation method thereof The invention discloses an acetylcysteine gargle for treating dental ulcers, and a preparation method thereof. The preparation method comprises the following steps: cooling a small amount of purified water by mass percent; adding the acetylcysteine and then stirring and mixing; under a stirring action, regulating the pH value until the acetylcysteine is dissolved; adding a solution stabilizer, a corrigent and a corrosion remover and mixing; adding poloxamer and then stirring till dissolving; statically placing an obtained mixture; filtering the mixture; and adding the water to a filtrate, thereby obtaining the acetylcysteine gargle. The acetylcysteine gargle prepared by using the method has the functions of quickly relieving pain and preventing/treating the ulcers, and especially has the medicinal efficacy of inhibiting the continuous ulcer expansion and promoting the ulcer wound healing for patients accepting radiotherapy, chemotherapy and bone marrow transplantation. The method provided by the invention has the advantages of simple preparation process and easiness in industrial scale production realization. The acetylcysteine gargle provided by the invention has the advantages of high stability, single and clear active ingredients and good quality controllability, thereby enriching the drug category for adjuvant therapy of clinical cancer. Therefore, a good selection for the nursing service of the patients accepting the radiotherapy is provided.
US20110027327 Cosmetic or pharmaceutical composition for topical application A cosmetic or pharmaceutical composition, to be applied topically is described, which has a hydrophilic outer phase, at least one cosmetic and/or pharmaceutical active ingredient and at least one carrier substance for the active ingredient. The carrier substance here forms such structures, which comprises at least two lamellar double membrane layers arranged one over another in the manner of a sandwich, wherein between adjacent double membrane layers, aligned parallel to each other, a layer of an inner phase is respectively arranged. The active ingredient is distributed in the double membrane layer and in the layer of the inner phase such that the layer of the inner phase contains the active ingredient in a concentration range between 2% by weight and 98% by weight and the double membrane layer contains the active ingredient in a concentration between 98% by weight and 2% by weight, respectively in relation to the total concentration of active ingredient, and the outer phase has no or almost no active ingredient.
CN103463051A Application of Lycojaponicumin A in medicaments for treating nasopharyngeal cancer The invention discloses application of Lycojaponicumin A in preparation of medicaments for treating nasopharyngeal cancer and belongs to the technical field of new application of medicaments. In-vitro methyl thiazolyl tetrazolium (MTT) anti-tumor activity evaluation discovers that the Lycojaponicumin A has a prominent inhibiting effect on growth of human nasopharyngeal cancer cell strains HNE1, HNE2, HONE1 and CNE1. Therefore, the Lycojaponicumin A can be used for preparing anti-nasopharyngeal cancer medicaments and has a good development and application prospect. The application of the Lycojaponicumin A in preparation of the medicaments for treating the nasopharyngeal cancer is made public for the first time; and because the skeleton type is completely novel, the Lycojaponicumin A has an unexpectedly strong nasopharyngeal cancer cell inhibiting activity.
CA2224217C Pharmaceutically active carotenoids The carotenoids lutein and zeaxanthin are disclosed for pharmaceutical use in the treatment of advanced macular degeneration. High dosages are deployed to produce the high serum carotenoid levels needed to cause take-up by the macula.
WO2012154354A1 Cgrp receptor antagonists The disclosure generally relates to the novel compounds of formula (I), including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).
CN103656373A Method for treating poultry eczema through herbal medicines The invention discloses a method for treating poultry eczema through herbal medicines. According to the method, 10-30g of radix scrophulariae, 5-20g of rhizoma smilacis glabrae, 5-15g of bunge corydalis herb, 5-15g of common goldenrod herb, 5-15g of flos chrysanthemi indici, 5-15g of radix scutellariae, 5-15g of cortex phellodendri, 5-12g of pericarpium citri reticulatae, 5-10g of honeysuckle flower and 5-10g of radix glycyrrhizae are decocted; the amount of the decoction is the dosage for 10 piglets; the decoction is fed one dose per day and is continuously fed for three days. 20-50g of fructus forsythiae, 20-50g of slender dutchmanspipe root, 20-40g of rhizoma smilacis glabrae, 20-40g of divaricate saposhnikovia root, 20-40g of herba schizonepetae, 20-40g of radix puerariae, 10-25g of cortex phellodendri and 15g of gypsum are ground and mixed with a feed for feeding.
CN102552268A Medicinal preparation containing crystal form a imatinib mesylate The invention discloses a medicinal preparation containing crystal form a imatinib mesylate. The medicinal preparation comprises crystal form a imatinib mesylate, a disintegrating agent, a diluent, a lubricating agent and a flow aid, wherein the using amount of the imatinib mesylate accounts for 50-80 percent of the total weight of the medicinal preparation; the using amount of the disintegrating agent is 15-30 percent of the total weight of a tablet; the using amount of the diluent is 0-20 percent of the total weight of the tablet; the using amount of the lubricating agent is 0.1-2 percent of the total weight of the tablet; and the using amount of the flow aid is 0.1-2 percent of the total weight of the tablet. Due to the adoption of the medicinal preparation prepared in the invention, the defects of poor flowability of a crystal form a and difficulty in preparing a solid preparation can be well overcome, the prepared medicinal preparation is dissolved quickly, and the crystal form does not change in preparing and storing processes.
US7041688 Alkynly-substituted spirocyclic sulfamides for the treatment of alzheimer's disease Compounds of formula (I) are disclosed. The compounds inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease
WO2006035760A1 Drug for treating skin disease Disclosed is an urea compound having a structure represented by the general formula [1] below which has a new pharmacological effect. The urea compound having the structure represented by the general formula [1] below or a salt thereof has an excellent curative effect on skin diseases. In the formula below, A represents -(NR4)-, -(CR5R6)- or -O-; B represents an alkylene or alkenylene group; R1, R2, R4, R5 and R6 respectively represent a hydrogen atom, an alkyl group, an alkenyl group, an adamantylalkyl group or the like; R3 represents an aryl group or an unsaturated heterocyclic ring; and X represents an oxygen atom or a sulfur atom.
WO2008130630A3 Polymorphic form of rimonabant hydrochloride and processes for preparation thereof Provided is a crystalline form of Rimonabant hydrochloride, processes for its preparation and pharmaceutical compositions containing such crystalline form of Rimonabant hydrochloride.
EP1427398B1 Device for the administration of an active agent to the human skin An article having an adhesive surface for adhering to human skin, said article comprising a first component constituting a continuos layer and at least a second component which is located in indentations in the adhesive surface of the first component without being in direct contact with the first component, said second component being separated from the first component by a cup shaped barrier layer, characterised in that the barrier layer is provided with a rim which extends into a flange.
CN1732951A Ceftriaxone sodium and tazobactam sodium composition The invention relates to a composition of ceftriaxone sodium and tazobactam sodium, which comprises active constituents of ceftriaxone sodium and tazobactam sodium by the weight ratio of 1-10:1, preferably 2-8:1, optimally 4:1. The compound preparation can appreciably reinforce the antibiotic action to Gram-negative bacteria.
CN103142568A Calcium acetate-vitamin K pharmaceutical preparation and preparation method thereof The invention relates to a calcium acetate-vitamin K pharmaceutical preparation and a preparation method thereof, belonging to the technical field of medicine. The calcium acetate-vitamin K pharmaceutical preparation is prepared from 400-1200 parts by weight of calcium acetate, 2-30 parts by weight of vitamin K and a right amount of auxiliary material, wherein the auxiliary material is selected from one or more of sucrose, microcrystalline cellulose, sodium carboxymethyl starch, micropowder silica gel, magnesium stearate, hydroxypropyl methylcellulose, talcum powder, lactose and mannitol. By using the scientific formula, the calcium acetate-vitamin K pharmaceutical preparation can effectively supplement calcium, and is safe and convenient to take.
CN101836992A Application of 4-benzothiopheneaminoquinazoline derivative in preparing tumor treatment medicine The invention discloses application of 4-benzothiopheneaminoquinazoline derivative and salt thereof in preparing tumor treatment medicine. The in vitro and in vivo activities of the 4-benzothiopheneaminoquinazoline derivative are evaluated; and the derivative kills tumor cells by means of inducing tumor cell apoptosis and autophagy to inhibit the growth of tumor cells and provide the application in preparing medicaments for treating cancers, especially pancreatic cancer, prostate cancer, lung cancer or breast cancer. In the invention, the action mechanism and the action target of the 4-benzothiopheneaminoquinazoline derivative are studied, and the derivative has stronger inhibitory activity to a plurality of receptortyrosinekinases and provides the application of acting as an inhibitor of receptortyrosinekinase, especially polyreceptortyrosinekinase.
CN100596294C 4'-substituted benzyloxy-phenyl butadiene derivatives and preparation and uses thereof The present invention provides a 4'-substituted benzyloxy -3',5'-dimethoxyphenyl-butadiene type derivatives and the medical salt or solvent thereof with the above general formula , wherein 4'-subsituted benzyloxy -3',5'-dimethoxyphenyl-benaldehyde and bromoethylcrotonate-triphenylphosphonium are mixed, and the mixture is reduced by a complex of lithium aluminium hydride and aluminium chloride to obtain the corresponding chemical compound. The chemical compound provided by the present invention has important biological activity, cytotoxicity experiments in vitro on human lung cancer cells (A549), human chronic myeloid leukemia cell Line (K562), human karyotype leukemia cell(HL-60), and mice lymph-type tumor (P388D1) tumor cells indicate that the derivatives of 4'-substrate benzyloxy -3',5'-dimethoxyphenyl-butadiene has the suppressive function on both the growth of tumor cells and multiple tumors in vitro, and can be applied to preparation of drugs for tumor prevention and treatment.
US6867222 Nociceptin analogs A compound of the formula (I), (II), (III) or (IV) wherein Z, A, B, C, R, R1, R2, Q, and n are as described herein.
EP2070550A1 Use of combinations comprising a corticosteroid and a pyrimidopyrimidine in the treatment of inflammatory diseases The invention features a method for treating a patient diagnosed with, or at risk of developing, an immunoinflammatory disorder by administering to the patient a tetra-substituted pyrimidopyrimidine, either alone or in combination with one or more additional agents. The invention also features a composition containing a tetra-substituted pyrimidopyrimidine in combination with one or more additional agents.
US6844466 Treating or preventing emphysema, cancer and dermatological disorders The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.
US20050175644 Preparation for oxidation-sensitive compounds and method for making same The invention concerns a method which consists in preventing oxidation of an active oxygen-sensitive compound of a medicinal and/or cosmetic formulation including at least a strong antioxidant and at least a weak antioxidant with high coating capacity, the strong antioxidant reacting with the oxygen before the active compound and the weak antioxidant reacting with the residual oxygen to form, after oxidation, highly coating particles which aggregate by micronization around the active compound to form a protective plaster. The invention is applicable in particular to compounds derived from 2,6-di-tert-butylphenol.
CN102232074A Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 ('mGluR2') and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
US20100203001 Process for forming disulfide bridges The present invention relates to an improved method of formation of disulfide bridges in substances bearing SH groups, in particular peptides, for example by formation of intramolecular disulfide bridges, in which a heterocyclic compound having at least one nitrogen atom (e.g. caffeine or a caffeine-like substance) is used for catalysis of the reaction. It was found, surprisingly, that addition of the heterocyclic substance increases both the yield and the purity of the product bearing disulfide bridges.
CN101926777A Method for preparing vidarabine monophosphate for injection The invention discloses a method for preparing vidarabine monophosphate for injection, which comprises the following steps of: dissolving vidarabine monophosphate into a solvent with heating, adding a proper amount of excipient and active carbon into the solution, filtering the solution to remove carbon, filtering the solution through a micropore filtration membrane, canning the filtrate into a tubular furbenicillin bottle, and putting the furbenicillin bottle into a freeze drier to perform freeze drying. The method is easy for industrialized production, solves the problem of vidarabine monophosphate freeze drying preparation, and ensures stable product quality.
US6921540 Hypotonic brines comprising mixtures of sodium, potassium, magnesium, calcium, chlorine and sulfates in water, used for prevention of inflammation of mucous membranes and for dissolving plugs in ears The present invention provides novel hypoosmotic saline compositions and their use as medicines for the prevention of the release of chemical mediators responsible for triggering phenomena causing inflammation of mucous membranes, and for the dissolution of cerumen plugs located in the external auditory meatus.
US20120214767 Tricyclic heterocyclic compounds Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
WO2013064919A9 Quinazoline derivatives with hsp90 inhibitory activity Compounds of general formula (I): or a stereoisomer, tautomer, polymorph, hydrate, solvate, or a pharmaceutically acceptable salt thereof, wherein R is as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as proliferative diseases, e.g. cancers, viral and fungal infections, neurodegenerative or inflammatory diseases or conditions. The invention also relates to the preparation of these compounds as well as to pharmaceutical compositions comprising them.
US20100247553 Goodpasture Antigen Binding Protein The present invention provides isolated nucleic acid sequences and expression vectors encoding the Goodpasture antigen binding protein (GPBP), substantially purified GPBP, antibodies against GPBP, and methods for detecting GPBP.
US7074770 Administering to a mammal a vector or nucleotide sequence which code an antigenic peptide; together with Schiff base A method of vaccinating a mammal against a disease state, comprising administrating to said mammal, within an appropriate vector, a nucleotide sequence encoding an antigenic peptide associated with the disease state; additionally administering to said mammal a compound which enhances both humoral and cellular immune responses initiated by the antigenic peptide, the compound being selected from the list contained herein, wherein the compound is preferably Tucaresol or a physiologically acceptable salt or ester thereof, where appropriate.
CA2284551C New therapeutic combinations of mirtazapine and antipsychotic agents, for the treatment or prophylaxis of psychotic disorders The present invention relates to therapeutic combinations of mirtazapine and an antipsychotic agent, to pharmaceutical compositions containing said combinations and to their use in the treatment or prophylaxis of psychotic disorders.
CN101863870A Tectorigenin derivatives, and preparation method and application thereof in treating prostatic diseases The invention relates to the field of natural medicinal chemistry, in particular to tectorigenin derivatives (I). R is defined as the specification. The derivatives and pharmaceutically acceptable salts thereof have good water solubility and can be used for improving or treating the diseases such as prostatic hypertrophy and/or chronic prostatitis and the like.
CN1575795A Naloxone hydrochloride nasal spray The present invention is nasal cavity spray of Naloxine hydrochloride and its preparation process. The preparation of the present invention may be applied in single dosage form or multiple dosage form. The spray of the present invention includes Naloxine hydrochloride, osmotic pressure regulator, preservative, osmotic promoter and water.
EP2667715A1 Treatment of autism spectrum disorderes using glycyl-l-2-methylprolyl-l-glutamic acid This invention provides compounds, compositions and methods for treating Autism Spectrum Disorders (ASD) using glycyl-2-methylprolyl-glutamic acid (G-2-MePE) and analogs thereof. Autism Spectrum Disorders include Autism, Autistic Disorder, Asperger Syndrome, Childhood Disintegrative Disorder, Pervasive Developmental Disorder - Not Otherwise Specified (PDD-NOS), Fragile X Syndrome, and Rett Syndrome. Compositions containing compounds include water-soluble formulations, water-in-oil micro-emulsions, water-in-oil coarse emulsions, water-in-oil liquid crystals, nanocapsules, tablets, and orally administered gels. The compounds and compositions of this invention can be administered intravenously, intraventricularly, parenterally, or orally, and can be effective in treating neurodegeneration, promoting neurological function, treating seizure activity and other symptoms of ASD, and can prolong life in animals including human beings having Autism Spectrum Disorders.
CN101623298B Preparation method of sodium ascorbyl phosphate oral solution The invention relates to the field of oral purgative prescription, in particular to a preparation method of sodium ascorbyl phosphate oral solution, comprising the following steps: raw material is dissolved, boiled and sterilized, and filtered and disinfected, the step of boiling and sterilization is that sodium benzoate with 0.02-0.03 percent of mass-volume ratio is added in the solution obtained in the step of the dissolution of the raw material, the solution is evenly stirred and is heat-insulated for 1-2 hours at the temperature of 98-100 DEG C; the step of the filtering and disinfection is that the boiled and sterilized solution is cooled to below 40 DEG C, essence with 0.10-0.13 percent of mass-volume ratio is added, and then the solution is filtered with a 0.22mum of a microfiltration membrane for obtaining the sodium ascorbyl phosphate oral solution. The total bacterial count in microorganism of the solution obtained by the invention is extremely low, thereby reducing the stimulation of the solution to intestinal canals.
EP1752161A2 Pulmonary surfactans comprising a polymyxin for improving the surface properties This invention is directed to pulmonary surfactants comprising additives for improving their surface tension lowering properties, and to the use of additives for improving the properties of modified natural surfactants or reconstituted/artifcial surfactants. More particularly this invention is directed to the use of polymyxins for increasing the resistance to inactivation of modified natural surfactants or reconstituted/artificial surfactants and/or increasing their activity.
CN102973532A Stable montelukast sodium tablet and preparation method thereof The invention relates to a stable pharmaceutical composition containing montelukast or salt of the montelukast and a method for preparing the composition. The montelukast sodium is easily affected by moist heat and light and degraded into sulfoxide and cis-isomer, so as to become a problem for development of a pharmaceutical preparation. A stabilizer is added to the stable montelukast sodium tablet disclosed by the invention to coexist with the montelukast sodium. Therefore, increase of the sulfoxide and the cis-isomer can be restrained to the maximal extent.
US20100210596 Use of aminopyrimidine compounds in the treatment of immune disorders The present invention provides methods of treating immune disorders. The present invention provides methods of treating an autoimmune disorder; methods of reducing the risk of transplant rejection; methods of increasing transplant survival; and methods of treating graft-versus host disease. The methods generally involve administering to an individual in need thereof an effective amount of an aminopyrimidine compound.
WO2009038107A1 Combined pharmaceutical preparation for treatment of type-2 diabetes Disclosed is a pharmaceutical preparation comprising a combination of mitiglinide (which is a substance useful for the treatment of type-2 diabetes) or a pharmacologically acceptable salt thereof and pioglitazone or a pharmacologically acceptable salt thereof. Also disclosed is a combined pharmaceutical preparation in which the therapeutic effect of pioglitazone or a pharmacologically acceptable salt thereof on type-2 diabetes can be enhanced in a patient in whom the blood glucose level cannot be sufficiently controlled by the administration of pioglitazone or the pharmacologically acceptable salt thereof alone, and in which the adverse side effects caused by the components contained therein cannot be increased synergistically. Thus, specifically disclosed is a pharmaceutical preparation for the treatment of type-2 diabetes, which comprises a combination of mitiglinide of the formula (Ia) or a pharmacologically acceptable salt thereof and pioglitazone of the formula (IIa) or a pharmacologically acceptable salt thereof.
WO2014005721A1 Use of (r)-phenylpiracetam for the treatment of parkinson's disease The present invention relates to the efficient treatment of an individual afflicted with Parkinson's disease (PD), the instant treatment comprising administering to the individual an effective amount of (R)-phenylpiracetam or a pharmaceutically acceptable salt thereof.
EP2489348A1 Pharmaceutical composition containing medicament-containing fine particles and method for producing same It is an object of the present invention to provide a pharmaceutical composition that can be used for an efficient administration of a water-soluble polymer drug by a method other than injection, and a method for production of the pharmaceutical composition. The above-mentioned object is achieved by a pharmaceutical composition comprising a small particle comprised of (a) a water-soluble drug and (b) a pharmaceutically acceptable ionic crystalline compound which is solid at room temperature, wherein the ionic crystalline compound is crystallized in the small particle.
CA2827577A1 A formulations comprising omega 3 fatty acids and an anti obesity agent for the reduction of body weight in cardiovascular disease patients (cvd) and diabetics Combinations of one or more anti-obesity drugs with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight comprised of a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DP A) and Docosahexaenoic acid (DHA) in a weight ratio of EPA: DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA comprise about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught. EPA + DHA are about 80% of the total formulation and about 89% of the total omega 3 fatty acid content of the composition. The formulation may further contain specific amounts of arachidonic acid (AA) and of omega-3 fatty acids having 18 carbon atoms, including one or more of stearidonic acid (SDA) and alpha-linolenic acid (ALA). The application further teaches methods of administering such combinations, and is directed towards unit dosages of such combinations for the reduction of body weight in cardiovascular disease patients (CVD) and diabetics.
CN103071149A Collagen and squalane composition, preparations thereof, and preparation methods and applications of composition and preparations The invention relates to a collagen and squalane composition. The composition comprises 0.1-20 parts by weight of collagen, 0.1-30 parts by weight of squalane and 1-150 parts by weight of a pharmaceutically acceptable carrier. The invention also relates to preparations containing the collagen and squalane composition, and a preparation method and an application of the composition. The collagen and squalane composition has the advantages of high biological availability, excellent curative effect, good stability, carrying and use convenience and the like.
WO2009151646A2 Non-invasive diagnostic agents and methods of diagnosing infectious disease The present invention is directed to novel non-invasive diagnostic tools to diagnose numerous infectious disease states or conditions. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these disease states. The novel imaging probe is capable of detecting infected cells, as well tissue. This represents a quantum step forward in the diagnosis and staging of NHL using non-invasively molecular imaging techniques. This novel probe will also be useful to monitor patients response to therapeutic treatments and other interventions or therapies used in the treatment of these disease states or conditions. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states. Pharmaceutical compositions are also described.
US7005526 Thioether derivatives Objects of the present invention are the compounds of formula (I) formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
US20060148897 Method for sterilization using in situ gelling materials A method for sterilizing a female or male patient is provided. The method comprises introducing into a reproductive duct of the patient a composition comprising a nucleophilic component, such as a thiol, and a component containing a conjugated unsaturated bond, such as an acrylate. The composition crosslinks within the reproductive duct. Within a female patient, the composition is introduced into one or both uterine tubes. The composition gels in the uterine tubes, thereby blocking the uterine tubes and preventing conception.
WO2011151651A1 Benzodiazepine compounds useful for the treatment of hepatitis c The invention concerns benzodiazepine derivatives of Formula (I) wherein A, X, L1, L2, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection.
US20120156305 Methods for enhancing genome stability and telomere elongation in embryonic stem cells The disclosure provides methods for increasing genome stability of an embryonic stem (ES) cell or induced pluripotent stem (iPS) cell, increasing telomere length in an ES or iPS cell, or both, for example by contacting an ES or iPS cell with an agent that increases expression of Zscan4 in the cell. Methods for increasing the genome stability in a population of ES or iPS cells, increasing telomere length in a population of ES or iPS cells, or both, are provided, for example by selecting Zscan4+ ES or iPS cells from the population of ES or iPS cells (which can include both Zscan4+ and Zscan4− ES or iPS cells). Therapeutic methods of using ES or iPS cells expressing Zscan4 are also provided. Further provided are methods of treating cancer by administering a Zscan4 polynucleotide or Zscan4 polypeptide. Also provided are methods of inducing differentiation of isolated ES or iPS cells into germ cells.
EP1333810B1 Oral dosage self-emulsifying formulations of pyranone protease inhibitors A microemulsion of pyranone protease inhibitor compounds that is substantially free of alcohol and propylene glycol comprising a pyranone protease inhibitor, one or more pharmaceutically acceptable surfactants, and a polyethylene glycol solvent having a mean molecular weight of greater that 300 but lower than 600, and a lipophilic component comprising medium chain mono- and di-glycerides, and optionally a basic amine.
US20130316974 Oxidized regenerated cellulose hemostatic powders and methods of making The present invention is directed to hemostatic material containing compacted ORC powder comprising particles having an average aspect ratio from about 1 to about 18, wherein said compacted ORC powder have preferably been processed in a compaction device, such as a ball milled ORC powder. The present invention further relates to methods of making the hemostatic material and a method of treating a wound by applying the hemostatic powder onto and/or into the wound of a patient.
WO2006024121A1 Use of n-phenylpiperazine derivatives and pharmaceutical compositions containing them This invention covers new N-phenylpiperazines derivatives and pharmaceutical compositions encompassing them, with these new structural clozapine derivatives ab a to act in dopamine andlor central-action pathways; these compounds were demonstrated to be useful in the treatment of erectile dysfunction and also useful as antipsychotics, with the advantages of not causing the side-effects typical of clozapine; they result in a lower incidence of catatonia when compared with haloperidol, another antipsychotic agent, and did not present any depressor effect on the central nervous system; the molecules also presented a hypothermic effect, which may be useful in the treatment of conditions presenting hyperthe~mia.
WO2008156365A1 Treatment of meconium aspiration syndrome with estrogens One aspect of the present invention relates to the use of an estrogen in the treatment of Meconium Aspiration Syndrome (MAS) in a newborn infant,said treatment comprising administering an effective amount of estrogen to said newborn infant within 7 days after birth. The present treatment offers the advantage that estrogens can be administered using non-invasive modes of administration, e.g. oral or rectal administration. Other aspects of the present invention relate to a suppository for use in newborn infants comprising at least1 μg of estrogen and to an oral applicator comprising a container holding an aqueous liquid containing micronised estetrol and a metering dispenser for metering the liquid into the oral cavity of a newborn infant.
US20090163577 METHODS AND COMPOSITIONS FOR ANTAGONIZING ANTI-APOPTOTIC Bcl-2-FAMILY PROTEINS The cytotoxic natural product gambogic acid (GA) competes for BH3 peptide binding sites on several anti-apoptotic members of the Bcl-2 family of proteins and neutralizes the ability of these proteins to suppress release of apoptogenic proteins from isolated mitochondria. Structure-function analysis of GA using analogs suggested a general correlation between BH3 competition and cytoxicity activity. Compositions and methods are provided for using GA and its derivatives for treating cancer and for discovering other compounds that are useful for treating cancer through their interaction with Bcl-2-family proteins.
CN103405416A Application of Chukrasone B in medicine for treating endometrial cancer The invention discloses application of Chukrasone B in preparation of a medicine for treating endometrial cancer, and belongs to the technical field of new application of medicines. The in-vitro MTT (3-4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) antitumor activity evaluation shows that Chukrasone B has remarkable inhibition effect on the growth of human endometrial cancer cell lines ISK and RL95-2, so that Chukrasone B has a good development and application prospect and can be applied to the preparation of the medicine for treating endometrial cancer. The application of Chukrasone B in the preparation of the medicine for treating endometrial cancer is disclosed for the first time; the framework type of Chukrasone B is brand new; Chukrasone B brings unexpected inhibition activity for endometrial cancer cells.
CN101433721A Nimesulide-hydroxypropyl-beta-cyclodextrin inclusion compound eye drops and preparation method thereof The invention discloses a nimesulide inclusion eye drop and a preparation method thereof. Nimesulide and hydroxypropyl-beta-cyclodextrin are prepared into an inclusion to improve the water solubility, and the inclusion of the nimesulide inclusion eye drop has the advantages of simple preparation technology, short production period, no residue of an organic solvent and so on. The nimesulide is prepared into a hydroxypropyl-beta-cyclodextrin inclusion solution eye drop or a solid powder eye drop, the solid powder eye drop is matched with water for injection before the use, and various additives can be added to the eye drop. The eye drop has small irritation, high stability, better eye anti-inflammatory and analgesic effects, and broad market prospect.
CN102525913A Separated water suspension medicine composed of hydrocortisone butyrate and water containing accessories and used for treating dermatosis The invention discloses a separated water suspension medicine composed of hydrocortisone butyrate and water containing accessories and used for treating dermatosis. The independently packaged hydrocortisone butyrate with D90 particle size of 0.1-10mu m and the independently packaged water containing one or several skin medicinal accessories together form the independently packaged water-insoluble skin medicine with the D90 particle size of 1-10mu m preferably, wherein the particle shape is sphere or similar sphere.
US20060069133 Administering a composition consisting of 2-ethoxy-1-[[2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid, a prodrug thereof or a salt thereof, a PPAR gamma agonist-like substance; diabetes, obesity The invention provides a pharmaceutical agent containing a compound having an angiotensin II antagonistic activity, a prodrug thereof or a salt thereof, which shows superior effect for the suppression of body weight gain. In addition, the present invention provides such a pharmaceutical agent as does not increase body weights of patients even if a therapeutically effective PPARγ agonistic substance is administered in the treatment of diabetes and other diseases.
CA2171836C Crystalline anhydrous mycophenolate mofetil and intravenous formulation thereof The crystalline anhydrous compound of formula (I) wherein the compound is complexed as a salt with an anion selected from the group consisting of chloride, sulfate, phosphate and acetate, in particular the hydrochloride salt, and compositions, intravenous formulations, and a kit thereof.
CN103070860A Anti-inflammatory analgesic composition and application thereof The invention provides an anti-inflammatory analgesic composition and application thereof, and belongs to the field of anti-inflammatory analgesic medicines. The anti-inflammatory analgesic composition contains indomethacin and buprofen, and can reduce toxic and side effects of the indomethacin on a gastrointestinal tract, without change of the anti-inflammatory analgesic effect. Through a large number of animal experimental models for screening, from different aspects, such as effectiveness and safety, great advantages of the indomethacin after formulation in the aspects of pharmacodynamics and safety are proved at the same time; a new composition is provided for clinical application of an anti-inflammatory analgesic medicine; and usually, the prepared anti-inflammatory analgesic composition can be prepared into granules, a tablet, a capsule, a syrup, a suppository, injection and the like by mixing a physiologically acceptable carrier body, an excipient, a binder, a diluting agent and the like.
WO2006025378A1 Remedy for hyperlipemia A remedy for hyperlipemia and hypercholesterolemia characterized by containing ezethimibe together with pitavastatine, a pitavastatine salt or a pitavastatine lactone.
US8628759 Soft anticholinergic esters Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X− is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
CN101579337A Clopidogrel composition and preparation method thereof The invention relates to a clopidogrel composition and a preparation method thereof, in particular to an active component clopidogrel with excellent effect of inhibiting platelet aggregation and a method for preparing a salt preparation thereof. The composition comprises the following components by mass portion: 1 portion of the clopidogrel, 4.5 to 30 portions of cyclodextrin, 1 to 10 portions of excipient and 10 to 100 portions of water for injection. The method comprises the following steps: adding the cyclodextrin represented by beta-cyclodextrin and derivatives thereof into clopidogrel alkaline solution; or dissolving the cyclodextrin and the derivatives thereof in the water for injection, and then adding the clopidogrel alkaline solution to the mixture, or mixing or ultrasonic or vacuum drying the mixture to obtain a clopidogrel-cyclodextrin clathrate compound for preparing a clopidogrel preparation which makes preparations more stable and safer.
WO2007129522A1 Preparation produced by dry process Disclosed is a pharmaceutical composition comprising a fructose 1,6-bisphosphatase (FBPase) inhibitor, which has excellent drug dissolution property, drug content uniformity, mass uniformity, hardness and wear resistance. Also disclosed is a solid preparation comprising the step of formulating a composition comprising a fructose 1,6-bisphosphatase inhibitor into a preparation by a dry process.
CN103446147A Application of Lycojaponicumin C in cervical cancer treatment drug The invention discloses application of Lycojaponicumin C in preparation of a cervical cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Lycojaponicumin C also has remarkable inhabiting effect on growth of human cervical cancer cell strains HeLa, HeLa229, HCE1 and CaSKi. Therefore, the Lycojaponicumin C can be used for preparation of an anti-cervical cancer drug and has good development and application prospect. The application of the Lycojaponicumin C in the preparation of the cervical cancer treatment drug is disclosed for the first time. The skeleton type is a novel skeleton type, and the high cervical cancer cell inhibiting activity of the Lycojaponicumin C is previously unimagined.
US20110195907 Amino acid and peptide conjugates of amiloride and methods of use thereof The present invention provides compositions comprising amiloride amino acid and peptide conjugates. Efficient methods are also provided for administering the amiloride conjugates of the present invention for treating cancer or a central nervous system disease or disorder or for preventing or reducing ischemia-reperfusion injury. Further, kits are provided for the treatment of a central nervous system disease or disorder or for the prevention or reduction of ischemia-reperfusion injury using the amiloride conjugates of the present invention.
CN103720707A Medical use of polyaspartic acid The invention discloses the medical use of polyaspartic acid. The medical use of the polyaspartic acid is characterized in that the polyaspartic acid is used for preparing medicaments for preventing or treating magnesium ammonium phosphate stones. According to the medical use of the polyaspartic acid, double functions of inhibiting the growth of the magnesium ammonium phosphate stones and promoting the dissolution of the magnesium ammonium phosphate stones are realized by utilizing the polyaspartic acid; a key technology is provided for researching and developing the medicaments for preventing and treating the magnesium ammonium phosphate stones of human and pet cats and dogs; moreover, as a synthetic peptide, the polyaspartic acid is non-toxic, has high biocompatibility, and can be developed as an ideal medicament for treating stones.
US20100144664 Carbocyclic compounds and methods for treating emerging disease, including influenza and venezuela equine encephalitis virus The present invention relates to the use of carbodine and 5-F carbodine and analogs thereof for use in the treatment or prophylaxis of influenza, in particular the H5N1 strain of Avian Influenza A virus or “bird flu” strain of influenza as well as the treatment or prophylaxis of Venezuela equine encephalitis virus or VEE.
CN101836948A Nitro-brate-containing sustained-release solid preparation The invention relates to a pharmaceutical solid preparation taking nitro-brate as an active ingredient and a preparation method thereof. The nitro-brate pharmaceutical active ingredient and pharmaceutically acceptable excipients are mixed to form the sustained-release solid pharmaceutical composition, and then are made into tablets, capsules and other solid agents. The sustained-release preparation has no toxicity, no mutagenic,carcinogenic and teratogenic effects, reasonable production process design, good stability of the prepared preparation, and long shelf life.
CN102432646A Gentamycin Cla derivative and extracting separation method thereof The invention relates to a Gentamycin Cla derivative and an extracting separation method thereof. The derivative which is obtained by separating from etimicin sulfate has a structural formula shown in the specification. The invention also relates to a separation method of aminoglycosides.
CA2145641C Pseudo-adenovirus vectors Gene Therapy vectors, which are especially useful for cystic fibrosis, and methods for using the vectors are disclosed. In preferred embodiments, the vectors are adenovirus-based. Advantages of adenovirus-based vectors for gene therapy are that they appear to be relatively safe and can be manipulated to encode the desired gene product and at the same time are inactivated in terms of their ability to replicate in a normal lytic viral life cycle. Additionally, adenovirus has a natural tropism for airway epithelia. Therefore, adenovirus-based vectors are particularly preferred for respiratory gene therapy applications such as gene therapy for cystic fibrosis. In one embodiment, the adenovirus-based gene therapy vector comprises an adenovirus 2 serotype genome in which the E1a and E1b regions of the genome, which are involved in early stages of viral replication have been deleted and replaced by genetic material of interest (e.g., DNA encoding the cystic fibrosis transmembrane regulator protein). In another embodiment, the adenovirus-based therapy vector is a pseudo-adenovirus (PAV). PAVs contain no potentially harmful viral genes, have a theoretical capacity for foreign material of nearly 36 kb, may be produced in reasonably high titers and maintain the tropism of the parent adenovirus for dividing and non-dividing human target cell types.
US20110009382 Substituted Benzimidazoles, Benzothiazoles and Benzoxazoles Substituted benzimidazoles, benzothiazoles and benzoxazoles, processes for their preparation, pharmaceutical compostions containing these compounds and the use of these compounds for treating or inhibiting disorders or disease states mediated at least in part by bradykinin receptor 1 (BR1).
US20050080468 Methods and apparatus for treating diseased tissue Methods and devices for treating diseased tissue using ultrasound waves are provided. The ultrasound waves are not focused, and advantageously are administered in conjunction with radiation therapy and/or chemotherapy. The methods and devices provide controlled delivery of ultrasound, and are particularly effective in treating cancers of non-bony tissue such as the breast.
WO2007069932A1 Method for suppressing appetite and food intake The invention relates to method for suppressing appetite and food intake in a mammal in need thereof comprising a step of administering to said mammal an effective amount of water comprising from 99.76 to 99.99 molecular % of isotopologue 1H2160. Further, invention relates to medical food for suppressing appetite and food intake in a mammal in need thereof which comprises water comprising from about 99.76 to about 99.99 molecular % of isotopologue 1H2160. Further, invention relates to the use of water comprising from about 99.76 to about 99.99 molecular % of isotopologue 1H2160 for the manufacture of a medical food for suppressing appetite and food intake in a mammal in need thereof. Because of suppressing appetite and food intake, this invention is particularly useful for treating overweight and obesity in a mammal in need thereof. Preferably, the mammal is human.
US8202896 Compounds, compositions and methods for treating or preventing pneumovirus infection and associated diseases Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.
WO2014025958A3 Treatment of immune-related and inflammatory diseases Provided herein are methods of using compounds and compositions for modulating leukocytic activity, including activity of B cells and/or T cells monocytes, macrophages, and other lymphoid or myeloid-derived cell types, in immune-related diseases or inflammatory diseases. Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.
US8129370 Use of oxicam compounds The invention relates to the use of lornoxicam or analogues thereof which inhibit cyclo-oxygenase 1 and cyclo-oxygenase 2 (COX 1 and COX 2), cannot penetrate the blood-brain barrier under physiological conditions, and reduce the prostaglandin E2-induced induction of the amyloid-precursor-protein (APP), for producing a pharmaceutical composition for the treatment or prevention of Alzheimer's disease or arteriosclerosis.
US20100172881 Use of tailored recombinases for the treatment of retroviral infections The present invention is directed to a method for preparing an expression vector encoding a tailored recombinase, wherein said tailored recombinase recombines asymmetric target sites within the LTR of proviral DNA of a retrovirus inserted into the genome of a host cell and is useful as means for excising the provirus from the genome of the host cell. The present invention further relates to an in vitro-method of optimising the treatment of a retroviral infection of a subject and to the use of tailored recombinases for the preparation of pharmaceutical compositions for reducing the viral load in a subjected infected by a retrovirus.
CN101564537A 3, 5-dihydroxy-4-isopropyl diphenyl ethylene-ethyl bromoacetate-polyoxyethylene compound and synthetic method thereof The invention discloses a 3, 5-dihydroxy-4-isopropyl diphenyl ethylene-ethyl bromoacetate-polyoxyethylene compound, namely polyoxyethylene-di(acetic acid-4-isopropyl-5-hydroxy diphenyl ethylene-3-phenolic ester). The original medicine is 3, 5-dihydroxy-4-isopropyl diphenyl ethylene (tolylene maud); and the modifier is polyoxyethylene and the linker arm is ethyl bromoacetate. The synthetic method of the compound includes three reactions, namely esterification reaction, hydrolysis reaction and esterification reaction. Compared with the original medicine, the compound has enhanced water-solubility and stability; the internal medicine distribution is changed; the bioavailability is enhanced; the synthetic method is simple; the reaction condition is mild; and the cost is low, without numerous unpleasant experimental procedures. In the method, the 3, 5-dihydroxy-4-isopropyl diphenyl ethylene-ethyl bromoacetate-polyoxyethylene compound can be easily made.
CN1886127A Use of desoxypeganine for the treatment of schizophrenic psychoses Desoxypeganine, as a free base or as an acid addition salt, or a derivative of desoxypeganine, in so far as it is also an inhibitor substance for acetylcholinesterase and monoaminooxidase, can be used in the production of a medicament for the treatment of a schizophrenic psychosis.
CN102766111A 3,4-diaryl-1,2,5-selenadiazole derivative and its application The invention belongs to the technical field of medicine and relates to a 3,4-diaryl-1,2,5-selenadiazole derivative, the structure of which is as shown in the specification, wherein R1-R8 are respectively and separately hydrogen, hydroxy, halogen atom, nitro, amino, alkoxy alkoxyl, alkyl amino, dialkyl amino, acyl amino or benzyloxy group, or two adjacent substituents can be -OCH2O- so as to form five-membered ring, or two adjacent substituents can be -CH=CH-CH=CH- so as to form six-membered ring. The invention also provides pharmaceutically acceptable nontoxic salt formed by the derivative as shown in the above structural formula and a hydrate thereof. The pharmaceutically acceptable nontoxic salt contains salt formed by the derivative and acid. It shows through results of a pharmacological activity test that the derivative has a good tumor inhibitory activity and can be used in a tumor cell proliferation inhibitor for preparation of antitumor drugs.
US7348321 Flumazenil for the treatment of alcohol dependency The invention relates to the use of flumazenil in developing a drug used for the sequential administration of small quantities of flumazenil at short intervals, until a therapeutically effective quantity is administered to treat alcohol dependence.
CN102908353A Application of ursolic acid on preparation of anti-HCV (hepatitis C virus) medicine and reagent The invention discloses new application of ursolic acid on preparation of anti-HCV, namely application of the ursolic acid on preparation of an anti-HCV medicine and a reagent. The ursolic acid is capable of remarkably inhibiting the proliferation of the anti-HCV in a cell infection model, and the in vitro and intracellular activity inhibition experiments discover that a RNA polymerase NS5B depended by HCV RNA is a key target functioned by the RNA polymerase NS5B. The ursolic acid is extensively distributed in the plant kingdom, the source is abundant, the toxic and side effects are low, and the selecting indexes (CC50/IC50) of the ursolic acid are consistent to the currently used therapeutic ribavirin in an anti-HCVJFH1 repdouction experiment of a cellular level, therefore, the new application of the ursolic acid can be applied to preparing the anti-HCV medicine, the reagent and an inhibitor of the polymerase NS5B copied by the reagent, thereby having the important economical value, medical value and social benefit. The ursolic acid on preparation of the anti-HCV medicine and the reagent has better HCV research and potential in the therapeutic use.
CN101062024B Pronin medicinal composition and its preparing method The invention discloses a pharmaceutical composition of tiopronin and its preparing process, wherein the composition is prepared from the following raw materials: tiopronin 100-300, anti-oxidizing agent 2-10. liposome 100-400, vitamin C 100-300, sodium glutamate 400-1000. The invention also provides the process for preparing the pharmaceutical composition.
CN101978952A Method for preparing berberine hydrochloride liposome preparation The invention discloses a method for preparing a berberine hydrochloride liposome preparation, which comprises an active medicament loading method and thin film evaporation and high-pressure homogenization processes. The method comprises the following steps of: A, dissolving lecithin and cholesterol into an organic solvent by using ultrasonic waves to obtain white transparent solution; B, recycling the solvent under reduced pressure from the solution which is obtained in the step A, and after a thin film lipid material is formed on a bottle wall, pouring solution of citric acid in to ensure that the thin film lipid material is fully dissolved; C, allowing the solution obtained in the step B to pass through a microporous filter film to obtain blank liposomes; D, adding solution of berberine hydrochloride into the solution of blank liposomes which is obtained in the step C, and dissolving fully by using the ultrasonic waves; E, adding sodium bicarbonate into the solution which is obtained in the step D and dissolving and regulating the pH value of the solution; F, incubating the solution which is obtained in the step E at the temperature of between 20 and 80 DGE C to obtain yellow lipoid suspension; and G, performing homogenization on the lipoid suspension which is obtained in the step F for 0 to 2 hours. The obtained liposomes prepared by the method have a uniform particle size and high stability, and the biological availability of berberine hydrochloride liposomes is improved.
US7163952 Azole compound and medicinal use thereof The present invention relates to an azole compound represented by the formula [I] wherein W is S or O; R is —COOR7, —X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is —(CH2)m—X— (X is —N(R8)—, —C(R9)(R10)—, —CO— or —CO—N(R8)—); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is —(Y)s1-(A2)s-Z (Y is —O—, —S(O)t—, —N(R13)—, —N(R14)—CO—, —N(R14)—SO2—, —SO2—N(R14)— and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.
CN103613493A 4'-methoxyl chalcone compounds as well as preparation method and use thereof The invention relates to a preparation method and use of 4'-methoxyl chalcone compounds. The 4'-methoxyl chalcone compounds are prepared by the step of carrying out a condensation reaction on seven different para-substituted benzaldehyde as raw materials and 4-methoxyl acetophenone to generate a target product in the existence of alkali. The compounds can activate the activity of tyrosinase, and meanwhile increase melanin content in cells and can be used for clinically preparing medicines for treating leucoderma. In vitro tyrosinase activity test is carried out for the synthesized compounds, and tests on tyrosinase and melanin content in B16 melanoma cells are further carried out. The experimental results show that the compounds 2f and 2g have a certain effect of activating the activity of tyrosinase. The compound 2d has a better effect of activating the activity of tyrosinase. The compounds 2b, 2e, 2f and 2g have certain proliferation effects to tyrosinase and melanin content in B16 melanoma cells of mice in a low concentration range of 5-20mu g/ml.
EP2419146A1 Modulation of inflammatory responses by factor xi Disclosed herein are antisense compounds and methods for modulating Factor XI and modulating an inflammatory disease, disorder or condition in an individual in need thereof. Inflammatory diseases in an individual such as arthritis and colitis can be ameliorated or prevented with the administration of antisense compounds targeted to Factor XI.
WO2010066858A1 Methods for the treatment and the prognosis of cancer The invention relates to an inhibitor of IL4I1 for use in a method for treatment of cancer displaying IL4I1-expressing cells in the human or animal body, provided that said cancer is not follicular lymphoma. In another aspect, the invention relates to a method for determining the prognosis of a subject suffering from a cancer, provided that said cancer is not follicular lymphoma, comprising the step of detecting the presence of IL4I1 in a sample obtained from said subject, wherein the presence of IL4I1 indicates that the subject has a poor prognosis. The invention also relates to a method for determining the prognosis of a subject suffering from a follicular lymphoma, comprising the step of detecting the presence of IL4I1 in a sample obtained from said subject, wherein the presence of IL4I1 indicates that the subject has a good prognosis.
EP1815859A2 Halimide, a cytotoxic marine natural product, and derivatives thereof The present invention provides a substantially purified compound having structure (I) wherein R1 to R9 are defined; or a salt of the compound, and provides pharmaceutical compositions comprising a compound of the invention and a pharmaceutically acceptable carrier. The invention also provides methods of reducing or inhibiting mitosis of a cell by contacting the cell with a compound of the invention, which blocks the cell at the G2/M phase of the cell cycle. The invention also provides a method of reducing the severity of a pathology characterized, at least in part, by undesirable proliferation of a population of cells in a subject by administering to the subject a compound of the invention in an amount sufficient to reduce or inhibit proliferation of the population of cells.
EP1284737B1 Water soluble prodrugs of azole compounds Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula (I) wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.
CN102813672A Application of aluminum ammonium sulfate dodecahydrate in preparation of antitumor matrix metal protease inhibitors The invention discloses an application of AlNH4(SO4)2.12H2O in the preparation of antitumor matrix metal protease inhibitors. Compared with previous MMPs inhibitors, the AlNH4(SO4)2.12H2O disclosed in the invention has the advantages of strong inhibition activity to the MMPs, simple structure, low price and convenient obtaining.
US20080306040 Antibacterial amide macrocycles VII The invention relates to antibacterial amide macrocycles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially bacterial infections.
EP2147913A1 Styrylquinolines, their process of preparation and their therapeutic uses The present invention concerns new substituted styrylquinolines, their process of preparation and their therapeutic uses as integrase inhibitors and/or for the treatment and/or prevention of HIV.
WO2009080837A1 Medicament for the treatment of cancer of the pancreas The invention relates to a suspension of red corpuscles encapsulating asparaginase as a medicament for treating pancreatic cancer. It in particular concerns a therapeutic composition or medicament intended for the treatment of pancreatic cancer, containing an effective quantity of such a suspension of red corpuscles.
US8609662 3-(heteroaryl-oxy)-2-alkyl-1-aza-bicycloalkyl derivatives as alpha. 7-nachr ligands for the treatment of CNS diseases The present invention relates to 1-aza-bicycloalkyl derivatives of formula (I) wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.
WO2013175009A1 Ulipristal acetate for prevention and treatment of breast tumors The invention relates to the use of ulipristal acetate, or any of its metabolites, in preventing or treating a breast tumor in a patient, preferably a patient that carries a mutation in BRCA1 gene.
WO2010121128A3 Compositions and methods for treating or inhibiting liver injury The present invention relates to the discovery that acetylsalicylic acid (ASA or aspirin), salicylic acid (SA) and related salicylate esters and their pharmaceutically acceptable salts, when coadministered in effective amounts with a drug or other bioactive agent which typically (in the absence of the salicylate compound) produces significant hepatotoxicity as a secondary indication, will substantially reduce or even eliminate such hepatotoxicity. Favorable therapeutic intervention results from the use of the present invention having the effect of reducing hepatotoxicity associated with the administration of certain drugs and other bioactive agents and in certain instances of allowing the administration of higher doses of a compound which, without the coadministration, would produce hepatotoxicity which limits or even negates the therapeutic value of the compound. The invention also relates inter alia to methods of inhibiting or reducing the likelihood of liver injury secondary to hepatitis, cirrhosis and a number of other disease states and conditions and further may be used to reduce the likelihood of a patient at risk or treating a patient for inter alia hepatitis, cirrhosis, non-alcoholic fatty liver diseases (NAFLD), non-alcoholic steatohepatitis (NASH), cirrhosis and other disease states and conditions as otherwise described. Pharmaceutical compositions are also described.
WO2007104557A3 Novel heterocyclic nf-kb inhibitors The present invention relates to compounds of the general formula (Ih) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, (Ih) wherein A is NR2, S or O; R3a is H, OH, SH, NH2, -C(NR7)NR7'R8, -(CH2)paryl, -(CH2)PNR7R8, -C(O)NR7R8, -N=CR7R8, -NR7C(O)R8, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, alkoxy, alkylamino, hydroxyalkylamino, halogen, aryl, or heteroaryl; R3 is H, -C(0)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4' OR5', NH2, hydroxyalkylamino, alkylamino, alkoxy, cycloalkyl, hetero- cycloalkyl, hydroxyalkyl, or haloalkyloxy; X is NR2', O, or S; Z is N or CR2'.
US20100137336 Novel amido derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
EP2586462A1 Prophylactic or ameliorating agent for genetic diseases An object of the present invention is to provide a prophylactic or ameliorating agent for a genetic disease that is caused by a mutation in an exon of a gene and is capable of forming a functional truncated protein by skipping of the exon comprising the mutation. The prophylactic or ameliorating agent used in the present invention is a prophylactic or ameliorating agent for a genetic disease that is caused by a mutation in an exon of a gene and is capable of forming a functional truncated protein by skipping of the exon comprising the mutation, wherein the prophylactic or ameliorating agent contains a compound having a molecular weight of 1500 or lower.
CN101984960A Rizatriptan benzoate capsule and preparation method thereof The invention discloses a medicinal preparation rizatriptan benzoate capsule for treating migraine and a preparation method thereof. Every 10000 capsules are prepared from the following formulation constituents: 29-250g of rizatriptan benzoate, 20-400g of microcrystalline cellulose, 220-1100g of starch, 100-400ml of 10-20% polyvinyl pyrrolidone ethanol solution and 4-30g of magnesium stearate. The invention also provides a preparation method of the rizatriptan benzoate capsule. The capsule of the invention covers the foreign taste of the main medicine; release and absorption of the medicine are accelerated; medical particles in the capsule are not punched or molten, thereby overcoming some defects of tablets; after the capsule is taken orally, the medicine is directly dispersed in the gastrointestinal fluid and is moistened by the gastrointestinal fluid, thus the effective surface area is large; and the medicine has higher dissolving rate in the gastrointestinal fluid, can be better absorbed and has high bioavailability.
WO2013085016A1 Pyridone derivative and medicine containing same General formula (I): The present invention pertains to: a pyridone derivate or a salt thereof represented by general formula (I); or a medicine containing the pyridone derivative or salt thereof as an active ingredient. [In the formula, ring A, R1, R2, R3 and R4 are specific groups.]
US20090215849 High stability aqueous gels comprising metronidazole and methods for the preparation thereof A method for preparing highly stable aqueous gels based on metronidazole, well suited for treating such skin conditions as rosacea, acne and dermatitis, entails the successive steps of: (A) forming a solvent medium M comprising water and propylene glycol; (B) dissolving the metronidazole in this solvent medium M, and optionally diluting the medium obtained by addition of water, whereby a solution S of metronidazole is obtained; and thence (C) mixing the solution S obtained with a gelling polymer, in a sufficient amount to ensure gelling of the composition.
CN102670488A Rupatadine syrup composition and preparation method thereof The invention relates to the technical field of biomedicines, in particular to a rupatadine syrup composition and a preparation method thereof. The rupatadine syrup composition comprises one or more of glycerol, propylene glycol and polyethylene glycol which serve as a cosolvent. By the preparation method, the solubility of rupatadine in a syrup aqueous solution is improved, the solubility of the rupatadine in a needed dosage is achieved, and the produced rupatadine syrup composition has stability and pharmacological effect consistency. Compared with the conventional rupatadine tablet, the composition has the characteristics that the dosage is easy to regulate, and the composition is suitable for children, convenient to take, high in patient compliance and high in medicine absorption speed.
US20110053960 Method for treating pain syndrome and other disorders The present invention provides the use of certain compounds to treat peripheral or central pain syndrome and other disorders associated with the T-type calcium ion channels.
EP0870500B1 Anti-helicobacter pylori agent A drug composition which comprises a combination of 4-[4-(4-methylbenzyloxycarbonyl)phenyl]phenyl trans-4-guanidinomethylcyclohexanecarboxylate or an acid addition salt thereof and a cyclodextrin, especially β-cyclodextrin, and is suitable for removing or exterminating Helicobacter pylori; and a composite of the same.
CN1586471A Silibinin meglumine salt oral disintegration tablet preparation and its preparing method The present invention relates to one kind of orally disintegrated silibinin-meglumine salt tablet for protecting liver cell, stimulating the biological synthesis of protein inside liver cell, promoting recovery of damaged liver cell, resisting fibrillation, capturing free oxygen radical and inhibiting the deposition and infiltration of fat in liver, and its preparation. The orally disintegrated silibinin-meglumine salt tablet is prepared with silibinin-meglumine salt as main material, and through adding stuffing, disintegrating agent, corrective, flow assistant and other supplementary material, pressing into tablet and other steps. The present invention has the features of low production cost, fast disintegration, good taste, etc.
US20110251155 Methods of Using Diacerein as an Adjunctive Therapy for Diabetes The present invention provides methods of treating type II diabetes using combinations of diacerein or its derivatives with other antidiabetic agents. The methods may also allow improving glycemic control of type II diabetes patients and/or reducing side effects and/or cardiovascular risks of antidiabetic agents.
WO2008062740A1 Nitrogenated fused ring compound and use thereof Disclosed is a compound which has an inhibitory effect on URAT1 activity and is effective for the treatment or prevention of a disease associated with a high serum uric acid level such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, urinary calculus, renal dysfunction, coronary artery disease and ischemic heart disease. Specifically disclosed is a nitrogenated fused ring compound represented by the general formula [1''], a salt thereof, or a solvate of the compound or the salt. [1''] wherein each symbol is as defied in the description.
CN101791307A Application of 2-imino-phenylate-5-(2-hydroxy-benzyl)-1,3-thiazole-4-ketone in preparing anti-cerebral cancer medicaments The invention discloses application of compound 2-imino-phenylate-5-(2-hydroxy-benzyl)-1,3-thiazole-4-ketone in preparing anti-cerebral cancer medicaments. The compound has the obvious function of inhibiting the cell proliferation of cerebral cancers and resulting in apoptosis and provides a new prospect for developing the novel anti-cerebral cancer medicaments.
CA2550986A1 Drug and/or food supplement containing nisylen, cepa, eurphrasia, belladonna and/or mercurius solubilis The present invention relates to a drug and/or food supplement with antiviral effects, in particular for the preventive and/or therapeutic treatment of herpes labialis and/or herpes genitalis, and/or with antibacterial and/or immunomodulating and/or antiphlogistic effects and/or for the preventive and/or therapeutic treatment of affections of the prostate, containing Nisylen and/or Cepa and/or Euphrasia and/or Belladonna and/or Mercurius solubilis.
CN101307056B Linear furocoumarin derivates, preparation method and application thereof, pharmaceutical compositions containing the derivates The invention provides a linear furocoumarin derivate with a structure expressed by formula 1, a method for preparing the same, an application of the linear furocoumarin derivate and a drug composition containing the linear furocoumarin derivate. The linear furocoumarin derivate has an activating function to GLUT4 membrane transfer and protein expression, and can be used as drugs for treating diabetes mellitus and complicating diseases of the diabetes mellitus.
WO2009127815A1 Aminoalyl-imidazotetrazines for treatment of cancer The present invention relates to imidazotetrazines of Formula (I) and their use in the treatment of cancer.
CN102757448A Macrocyclic kinase inhibitor compound, preparation method and application thereof as drug The invention relates to a compound shown in a formula (I), wherein L, R1, Z, A, B and C are defined in the application specification. The invention also relates to the application of the compound shown the formula (I) as kinase inhibitors.
US20120136054 Materials and methods for measuring nitric oxide levels in biological fluids The subject invention presides novel devices and methods for the measurement of nitric oxide in biological samples, including wound fluid samples. These advantageous devices and methods can be used for clinicians to monitor the wound's nitric oxide metabolism and/or response to treatment.
CN1943738A A medicine for treatment of chronic nasosinusitis This invention relates to a kind of medicinal preparation which has the therapeutic function of chronic nasosinusitis. It is characterized in that the medicament is made up of some high grade raw materials including Lonicera japonica Thunb, Dendranthema morifolium, Magnolia liliflora, Fructus xanthii, Herba Menthae, Radix Angelicae Dahuricae, Manchurian Wildginger, Herba Taraxaci, Foliumisatidis, Houttuynia cordata, Ligusticum wallichii, Radix Angelica, Scutellaria, Semen Coicis Coix lachrymal, Gypsum Fibrosuum, Radix Glycyrrhizae and so on. All the raw materials are mixed according to the definite ratio of weight. The medicament is decocted and taken by oral administration. A dosage is taken in a day and fifteen days as a course of treatment. It is characterized in its high curative ratio, obvious therapeutic effectiveness, symptoms removed rapidly, non-toxic side effectiveness, lower cost of therapy, non-relapse and capable of eliminating pains radically. In all, the medicament can be used in therapy of chronic nasosinusitis effectively. According to clinical trial, the effective rate, the effectual rate and the cure rate of the medicament is up to 96.7%, 87.9% and 63.7%, respectively.
WO2013185766A1 Gpr120 receptor modulators There is provided novel compounds of formula (I) (insert formula (I)) capable of modulating the G-protein-coupled receptor GPR120, which can be used for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels. Also the compounds for use in the treatment of obesity type II diabetes and metabolic syndrome.
US20100120907 Derivatives of amyris alcohols and eudesmol for treating cold sores and herpes Provided are topical formulations comprising an Amyris alcohol and/or ester derivatives of Amyris alcohol which may be used for the treatment of diseases including herpes virus infection (e.g., HSV-1, HSV-2), epidermoid carcinoma, cold sores, and human papillomavirus. Amyris alcohols contemplated for use with the present invention include valerianol, beta-eudesmol, epi-gamma-eudesmol, elemol, alpha-eudesmol, and ester derivatives thereof.
US20080085296 Methods for reduction of post operative ileus. An apparatus and method for reducing post-operative ileus and/or gastric stasis is described. The method can include applying to the intestine a therapeutically effective amount of a composition comprising a drug that is effective in reducing post-operative ileus and/or gastric stasis, such as by introducing the composition through a surgical access device, such as a trocar or endoscope. The apparatus can include a sheet of material, a surgical fastener, or a buttress comprising the composition.
US20050080046 In liquid solvent; parenterally administering; aldosterone receptors blockers; congestive heart failure, hypotensive agents, liver disorders There is provided a parenterally deliverable pharmaceutical composition comprising eplerenone and a solvent liquid having the eplerenone in solution therein. Compositions of the invention are storage stable.
CN102580060A Medicine composition for curing diabetes mellitus and complications of diabetes mellitus The invention belongs to the field of pharmaceuticals, and specifically relates to a medicine composition for curing diabetes mellitus and complications of diabetes mellitus, in particular to a medicine composition containing insulin analogue and low molecular heparin or medicinal salts of insulin analogue and low molecular heparin. Compared with single dose, the medicine composition has remarkable superiority on improving blood sugar, urine sugar and glycated serum protein level of a glucose kinase (GK) rat, has good synergistic effect and has good synergistic effect on improvement of C-reactive protein (CRP) level and inhibition of complement C3 activation so that the medicine composition for curing diabetes mellitus and complications of diabetes mellitus can be used for preventing and/or curing diabetes mellitus and complications of diabetes mellitus.
US20100173884 Use of a phytosterol containing composition for the treatment of luts The invention relates to the use of a composition comprising an oil-extract and a water-soluble extract, wherein said extracts are obtainable from plant materials and said extracts comprise phytosterols, for the manufacturing of a medicament for the treatment of females suffering from LUTS as a consequence of Interstitial Cystitis and/or stress or urge incontinence.
CN1935157A Medical stone emulsifiable paste for treating skin disease and its preparing method The present invention relates to a wheat-ball stone emulsifiable paste for curing dermatosis and its preparation method. Its raw material composition contains the components of wheat-ball stone, zine oxide, iron vitriol powder and liquefied phenol. It has obvious therapeutic effect for curing the diseases of psora, eczema, dermatitis and other subacute and chronic pruritic dermatosis.
US8329731 PTEN inhibitor or Maxi-K channels opener A new PTEN opener or a new opener of a large conductance Ca2+-activated K+ channel (Maxi-K channel) which comprises as an active ingredient a tetrazolylalkoxy-dihydrocarbostyril compound of the formula (I): wherein R is cycloalkyl, A is lower alkylene, and the bond between 3- and 4-positions of the carbostyril nucleus is single bond or double bond, or a salt thereof, which is useful as a medicament for promotion of the survival of normal cells, brain cells, heart cells, and skin, and further for inhibiting of Gram negative sepsis and cell migration and cell invasion due to inhibition of PTEN and is further useful as a medicament for the treatment of neuronal disorders, for example, an anticonvulsant, a neuroprotecting agent, a medicament for treatment of regional cerebral edema and neurologic motor impairment, cognitive disorders, traumatic brain injury, Parkinson's disease, epilepsy, migraine, and Alzheimer's disease, etc.
WO2007049798A1 Novel benzoxathiin derivative Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzene ring or the like; X1 represents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; X2 represents a group represented by the following formula (II): (wherein R4 and R5 respectively represent a lower alkyl group or the like, and m represents a number of 2-4) or the like; one of X and Y represents an oxygen atom and the other represents a sulfanyl group or the like; and X3-X6 respectively represent -CH-, a nitrogen atom or the like.]
US7569688 Propane-1, 3-dione derivative Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.
EP1971230A2 Treatment of stressed patients Methods and compositions for providing nutrition to critically ill patients are presented. In an embodiment, the method comprises administering to a patient undergoing a condition characterized by a systemic inflammatory response phase followed by a compensatory anti-inflammatory response phase a first nutritional composition while the patient is experiencing the first phase and administering to the patient a second different nutritional composition while the patient is experiencing the second phase.
WO2009024022A1 Fatty acid bile acid conjugates and medical uses thereof Fatty acid bile acid conjugates of formula I, pharmaceutically acceptable salts, their preparation methods, pharmaceutical compositions containing the same, and the uses of the fatty acid bile acid conjugates or their pharmaceutically acceptable salts for preparing the drugs useful in the prophylaxis or treatment of gall-stone, fatty liver, atherosclerosis and so on, in which, R1 represents trans- or cis-OH, R2 represents H or OH, R3 represents H or C1-5alkyl, and n is an even number in the range of 4-20.
CN1634014A Sodium ferulate oral disintegrating tablet and its preparation process The invention discloses a sodium ferulate orally disintegrating tablet and its preparation, wherein the tablet is prepared by using sodium ferulate as raw material, using bulking agent, crumbling agent, flavoring agent, flow aid, and lubricating agent as adjuvant, using bonding agent or dressing material based on specific situation, or charging right amount of effervescent agent, then using specific preparing procedure and employing a tablet compressing machine for pelleting. The invention realizes quick disintegrating speed, good taste, the tablet can be taken under the condition of waterless, it has the advantages of fast effect, improved compliance for the patients, and increased curative effect of the medicament.
CN102370922A Powdery preparation for treating tinea pedis The invention discloses a powdery preparation for treating tinea pedis. The powdery preparation consists of lightyellow sophora root, sessile stemona root, rhubarb, salicylic acid, benzoic acid, boric acid, alum, menthol crystal, hibitane acetate, triclosan and talc powder. Disinfection and antisepsis components, i.e., hibitane acetate and triclosan serving as efficient disinfection and antisepsis medicament and having strong killing effects on fungi and the like are added into the conventional tinea pedis powder, so that mold fungi (fungi) causing tinea pedis can be killed effectively, and reoccurrence is prevented. The powdery preparation can be used for soaking feet by adding hot water, and can be directly applied to bullous type tinea pedis in a small amount.
US7022711 2-(4-Pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones This invention provides antiangiogenic compounds of the Formula (I), which are useful for treating diseases, resulting from uncontrolled cellular proliferation such as cancer, atherosclerosis, rheumatoid arthritis, and psoriasis.
CN102631363A Application of tectoridin in preparing medicine for preventing osteoporosis The invention relates to an application of tectoridin in preparing a medicine for preventing osteoporosis. Through the research on the influence of the tectoridin on osteoporosis samples of ovariectomized rats, the medicine can be proved to have the functions of slowing down the weight enhancement of the sample rats with osteoporosis, enhancing the bone mineral density value and the serum calcium and phosphor concentration values and improving the bone tissue measuring index, the tectoridin is proved to have the function of preventing and treating the osteoporosis, and the effect of the tectoridin is better than thatt of the same dosage of irigenin.
US7629354 Use of phanquinone for the treatment of Alzheimer's disease The use of phanquinone for the manufacture of a pharmaceutical composition for the prevention or the treatment of Alzheimer's disease is disclosed. Also methods of treatment or prevention of Alzheimer's disease are disclosed.
WO2008090327A1 New combination for use in the treatment of cancer There is provided combination products comprising: (a) a compound of formula (I), wherein X, Y, T, W, A1, A2 R1, R5 and R6 have meanings given in the description, and (b) trastuzumab or a tyrosine kinase inhibitor. Combination products according to the invention find particular utility in the treatment of cancer.
WO2012096887A2 Compositions comprising enzyme-cleavable oxycodone prodrug The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
US20080227808 5-{3-[3-Bromo-5-methylsulfanyl-2-(2-pyridin-3-yl-ethoxy)-benzylamino]-propylamino}-4H-thieno[3,2-b]pyridine-7-one; anti-Clostridium difficile agents Novel bicyclic heteroaromatic compounds are provided that are inhibitors of bacterial methionyl tRNA synthetase (MetRS). Compounds of the invention generally have a left hand side phenylether constituent and a right hand side thienopyridone constituent. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, particularly as anti-Clostridium difficile agents.
CN103242307A Crystal form I of oxazolidinone derivative as well as preparation method and application of crystal form I The invention relates to a crystal form I of (S)-5-Cl-N-((2-oxo-3-(4-(2-oxo-2H-pyridine-1-radical) phenyl)-1, 3-oxazolidine-5-radical) methyl) thiophene-2-formamide as well as a preparation method and application of the crystal form I. The prepared crystal form I of the (S)-5-Cl-N-((2-oxo-3-(4-(2-oxo-2H-pyridine-1-radical) phenyl)-1, 3-oxazolidine-5-radical) methyl) thiophene-2-formamide can be characterized through an X-powder diffraction pattern.
US20080058377 N-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-N'-[4-(trifluoromethyl)benzyl] urea; antiinflammatory agent: asthma or COPD, analgesic: neuralgia, neuropathies, algesia, nerve injury, ischemia, neurodegeneration, or stroke; urological diseases: urinary incontinence or overactive bladder This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
WO2004098634A3 Protein arginine n-methyltransferase 2 (prmt-2) The invention provides insight into the function of Protein Arginine N-Methyltransferase-2 (PRMT-2) and provides methods for modulating PRMT-2 activity or expression in cells. The methods of the invention can be used to inhibit the function of NF?B, E2F1 and STAT3 and have utility for treating a variety of conditions including, for example, inflammation, HIV infection, cancer and obesity.
US20050079148 Biocompatible polymer designed to release nitric oxide; extensively cross-linked polyamine-derivatized divinylbenzene; sustained release, potentiation Extremely hydrophobic nitric oxide (NO) releasing polymers are disclosed. The extremely hydrophobic NO-releasing polymers provided are extensively cross-linked polyamine-derivatized divinylbenzene diazeniumdiolates. These polymers can be loaded with extremely high NO levels and designed to release NO in manners than mimic natural biological systems. The NO-releasing extremely hydrophobic polymers provided can maintain a sustained NO release for periods exceeding nine months. Also provided are related medical devices made using these NO-releasing extremely hydrophobic polymers.
US20120076734 Radiopaque antibiotic dental paste and uses thereof Compositions useful for disinfecting a dental wound are described. The compositions include an active ingredient comprising one or more antibiotics, a radiopaque substance, and optionally a pharmaceutically acceptable excipient. Methods for treating dental wound sites with the compositions are also described.
CN102078298A Lansoprazole liposome combined medicament as well as preparation method and applications thereof The invention relates to a lansoprazole liposome combined medicament as well as a preparation method and applications thereof. The invention is characterized in that the mass industrial production of lansoprazole liposome combined medicament injections and the mass industrial production of lansoprazole liposome combined medicament oral preparations can be carried out by using a molecular dispersion method through uniform prescription, process and equipment. The invention provides a mol ratio prescription of various component raw materials for preparing the lansoprazole liposome combined medicament, provides the preparation steps, the method and the concrete embodiment for preparing lansoprazole liposome combined medicament freeze-dried injections and oral preparations. The lansoprazole liposome combined medicament provided by the invention is used for resisting gastric ulcer.
US20110015141 Method for treating cancers having high glucose requirements employing an sglt2 inhibitor and compositions thereof Methods are provided for treating cancers that have high glucose requirements and that express SGLT2 at levels higher than normal cells, such as metastatic cancers, for example, metastatic lung cancers, employing an SGLT2 inhibitor alone or in combination with a cytotoxic agent and to a composition containing a combination of an SGLT2 inhibitor and a cytotoxic agent.
US20120114759 Peptide/particle delivery systems Polymeric nanoparticles, microparticles, and gels for delivering cargo, e.g., a therapeutic agent, such as a peptide, to a target, e.g., a cell, and their use for treating diseases, including angiogenesis-dependent diseases, such as age-related macular degeneration and cancer, are disclosed. Methods for formulating, stabilizing, and administering single peptides or combinations of peptides via polymeric particle and gel delivery systems also are disclosed.
CN103110620A Catechin applied in detoxification body intaking PAEs type environmental endocrine disruptor The invention relates to a catechin applied in detoxification body intaking PAEs type environmental endocrine disruptor. Prepared into an oral solution and taken orally, the catechin disclosed by the invention has the advantages of good curative effect for the detoxification body intaking PAEs type environmental endocrine disruptor and good application prospect. Moreover, the dosage of the catechin is 10-50mg/kg.
WO2013084199A1 Boron heterocycles as new inhibitors of human neutrophil elastase The invention described herein provides a new family of human neutrophil elastase (HNE) inhibitors. These are boron heterocycles of the general formula shown in (I) and (II), wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined in the specification section as well as their isomers and racemates and their use as HNE inhibitors. The use of these compounds and also of the pharmaceutical compositions and medicaments containing them is useful in treating human HNE related diseases and is therefore applicable in both Pharmaceutical and Medical industries.
US7557105 Proliferative disorders; cancer; 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide The invention relates to N-phenyl-2-pyrimidine-amine derivatives in which at least one nitrogen atom carries an oxygen atom to form the corresponding N-oxides, to processes for the preparation thereof, to pharmaceutical compositions comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.
CN1739567A Dietotherapeutic nutrient for preventing and treating adipose hyperglycemia and slimming and its prepn process The dietotherapeutic nutrient for preventing and treating adipose hyperglycemia consists of purine nucleotide, compound vitamin, compound trace elements, compound mineral matter, essential fatty acid oil and proper amount of edible cellulose as stuffing and hypoglycemic. The dietotherapeutic nutrient is used as main material or additive for food products and medicines for preventing and treating diabetes through balancing insulin and hyperglycemic hormone, repairing the functions of pancreatic island and kidney, preventing and treating complication and restoring normal synthesis and metabolism. The present invention has c-GMP, trace elements, etc. to regulate second messenger c-AMP amount, lift, activity and release time of hyperglycemic hormone, calcium carbonate to buffer and neutralize flavone and other acid matter and acid poisoning, potassium citrate to replenish potassium and to maintain acid-alkali and electrolyte balance. The dietotherapeutic nutrient has no toxic side effect and dependence.
CN103720673A Nifedipine sodium alginate sustained release tablet The invention discloses a nifedipine sodium alginate sustained release tablet, and belongs to the field of medicine. The nifedipine sodium alginate sustained release tablet mainly comprises the following components in percentage by weight: 10 to 12.5% of nifedipine, 15 to 35% of sodium alginate, 30 to 50% of microcrystalline cellulose, 10 to 12.5% of sodium phosphate dodecahydrate and 10 to 12.5% of calcium hydrogen phosphate dehydrate. The nifedipine sodium alginate sustained release tablet has performance of slowly releasing nifedipine in vitro, and the content of the sodium alginate does not influence the tensile strength of the tablet, so that the nifedipine sodium alginate sustained release tablet is a good nifedipine sustained release dosage formulation.
EP1976851A2 Phenoxy-substituted pyrimidines as adenosine receptor antagonists Compounds of formula (I), including pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof thereof, wherein R1, R2, R3, R4, R5, X, m and n are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
WO2006025267A1 Remedy for sleep disorders using lowering in per2 protein level as the action mechanism It is intended to provide a drug which is useful in preventing and/or treating sleep disorders such as time zone change syndrome, shift work sleep disorder or circadian rhythm sleep disorder such as sleep phase delay syndrome, i.e., a preventive and/or a remedy for sleep disorders comprising a compound having an effect of lowering the PER2 protein level as the active ingredient.
CN1795853A Gelata of ornidazole A gel of ornidazole for treating the infection of anaerobic bacterium by applying it through skin or mucosa is prepared from or nidazole and different auxiliaries.
CN1846700A Slow-released 5-fluorouracil system in vitreous chamber The present invention provides one kind of slow released 5-fluorouracil system in vitreous chamber. The slow released 5-fluorouracil system has medicine carrying amount of 10.44%, medicine carrier of synthesized biodegradable polymer polylactic acid, and emulsifier of water soluble polymer PVA. The slow released 5-fluorouracil system is suitable for use after the surgical operation on vitreoretinopathy, and after being injected into vitreous chamber, it may maintain smooth medicine release for 28 days to inhibit the proliferation of active cell inducing proliferative vitreoretinopathy, block the acting path of the cell factors and prevent proliferative vitreoretinopathy effectively.
CN101525364A Crystal form of fulvestrant and preparation method thereof The invention discloses a novel crystal form of fulvestrant, a preparation method thereof and a pharmaceutical composition containing the crystal form.
CN102100803A Health-care product composite with alcoholism relieving function and preparation method thereof The invention relates to a health-care product composite with an alcoholism relieving function and a preparation method thereof, and discloses a health-care product composite with an alcoholism relieving function and a preparation method thereof. The composite is prepared from the following raw materials: pueraria flower, hovenia dulcis thumb, kudzuvine root, green tea and oligosaccharide, wherein plantain herb, chrysanthemum, lalang grass rhizome, liquoric root, tangerine peel and hawthorn fruit are also added into the raw materials of the composite. The health-care product composite is prepared by refining wild plants, does not have toxic or side effect, has excellent effects of relieving alcoholism and activating spleen and protecting liver and stomach, and can eliminate or relieve acute mild and moderate alcoholism, acute stomach injury, chronic gastritis and acute liver injury which are caused by drinking. The health-care product composite can be prepared into granules, tea bags and capsules.
WO2014023083A1 PI3Kδ INHIBITOR Disclosed are a PI3Kδ inhibitor compound of formula (I), pharmaceutically acceptable salts, stereoisomers or deuterated compounds thereof, preparation methods of these compounds, a pharmaceutical preparation containing these compounds, and the use thereof for preparing a medicine for treating inflammatory disorders or tumours.
US6953583 Use of conjugated linoleic acid (CLA) for the topical treatment of cellulite The present invention relates to the use of conjugated linoleic acid (CLA) for the topical treatment of fatty deposits and cellulite and to new topical compositions and to cosmetic and dermatological topical compositions for the treatment of fatty deposits and cellulite comprising CLA as well as kits comprising CLA for said treatment.
CN101342153B Risperidone osmotic pump controlled release tablets and preparation method thereof The invention relates to a risperidone osmotic pump controlled release preparation, which is composed of semipermeable film coating and a solid tablet core. The semipermeable film coating comprises coating materials and plasticizers; the solid tablet core comprises main drug, cosolvent, osmotic pressure accelerants, filling agents and lubricants. The invention also relates to a preparation methodof the risperidone osmotic pump controlled release preparation. The preparation has the characteristics of long efficacy, stable curative effect and few toxic and side effects, and the preparation process is simple and is easy for industrial production.
WO2007054748A1 Indole derivatives as antitumoural compounds Antitumoural compounds of general formula (I); wherein Ar is an heterocyclic group of formula (a) and R1, R2, R3, R4, R5, R6, R7, n and the dotted line take permitted meanings can be obtained from a tunicate of the family Polyclinidae, genus Aplidium, species cyaneum, and the invention further provides derivatives thereof.
US7332495 Aralkyl-ketone piperazine derivatives and their uses as new antalgic or ataractic agent Arylalkyl ketone piperazine derivatives of the formula: and pharmaceutical compositions comprising the same. Also disclosed are methods for using the compounds as analgesic and sedative agents. The compounds of the present invention have good analgesic and sedative activities but few side effects.
US20100197712 Use of dopamine stabilizers At least one embodiment of the present invention relates to the use of a dopamine stabilizing substance in an oral, subcutaneous or intramuscular daily dose of 1-20 mg or in an intravenous daily dose of 0.1-2 mg in treatment of a neurological or psychiatric disorder characterized by a hypofunction of the dopamine system. At least one embodiment of the invention also relates to the use of a dopamine stabilizing substance in an oral, subcutaneous or intramuscular daily dose of 25-50 mg in treatment of a disorder caused by instability of neural circuits.
WO2012123383A2 Buccodental hygiene and/or care composition The invention relates to a composition comprising chlorhexidine or one of the soluble salts thereof and sodium docusate (DOS S) in a chlorhexidine or one of its soluble salts / sodium docusate molar ratio equal to ½, in a hydroalcoholic vehicle comprising between 30 and 60 % of alcohol (v/v) in relation to the total volume of the composition. The compositions according to the invention are advantageous in that they extend the amtimicrobial activity of the chlorhexidine after use (improvement of the persistence) and reduce the phenomenon of blackening in the buccal cavity.
CN1602876A Dimethoxanate hydrochloride dripping pills and its preparation method The invention discloses a dimethoxanate hydrochloride pill prepared by superfine crushing and pill producing technique, and can achieve the purposes of increasing disintegration and dispersion speeds, quickly taking effect, improving drug stability, reducing auxiliary use, reducing production cost, being convenient to carry and take. Its compliance is good and especially suitable for children, the aged, patients in bed and patients difficult in swallowing to take.
CN101658487B Glimepiride aqueous solution administration system and preparation method thereof The invention relates to a glimepiride aqueous solution administration system and a preparation method thereof, which belong to the technical field of medicaments. A glimepiride aqueous solution preparation consists of an active component glimepiride and a pharmaceutically acceptable adjuvant, and each 100 milliliters of the preparation contains 0.1 to 10 grams of the glimepiride, preferably 0.1 to 5 grams, and most preferably 0.1 to 2 grams. The glimepiride aqueous solution administration system and the preparation method have the advantages of successfully solving the problem that the glimepiride is extremely difficult to dissolve, and greatly improving the stability of a solution through a series of prescription screening works. The system or a composition performs administration in a sublingual spraying mode to avoid the action of alimentary canals, the reactions of gastrointestinal tracts and the liver first pass effect; besides, the system or the composition has quick response and high bioavailability, is particularly suitable for controlling the postprandial blood sugar, and can be used for treating the type 2 diabetes which cannot be appropriately controlled by dietary restriction and sports. The system or the composition also has the following advantages that: the use is convenient, the dosage can be adjusted as required, the compliance is good, the system or the composition is particularly suitable for old people and the patients who cannot swallow conveniently, the preparation process is simple and practicable and is suitable for industrial production, and the like.
US20120108530 Enhanced Neoglycosides Through Neoglycosylation and Methods of Use Thereof Using neoglycosylation, the impact of differential glycosylation upon the divergent anticancer and anti-HIV properties of the triterpenoid betulinic acid (BA) was examined. Each member from a library of 37 differentially glycosylated BA variants was tested for anticancer and anti-HIV activities. Enhanced analogs for both desired activities were discovered with the corresponding antitumor or antiviral enhancements diverging, based upon the appended sugar, into two distinct compound subsets.
WO2008020799A1 Thienopyrimidin-4-one and thienopyridazin-7-one derivatives as mch rl antagonists The claimed invention provides thienopyrimidin-4-one and thienopyridazin-7-one MCH Rl antagonists, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds of Formula (I) may be used for treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, type II diabetes, Metabolic syndrome and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders.
US20140073598 Multiple folate formulation and use thereof A multiple folate composition having at least 3 different forms of folate comprising at least one of folic acid (a salt or ester thereof); at least one of a folinic acid (a salt or ester thereof); and at least one of a 5-methyl-tetrahydrofolic acid (a salt or ester thereof) is disclosed. The composition is useful as a nutritional supplement or medication in the treatment of folate deficiency and the sequella thereof and/or in conditions responsive to administration of metabolically useful folate. The compositions are particularly of use in patients who have impaired or reduced ability to convert folic acid to its metabolically active forms, and in the treatment of depression.
EP1317262A4 Topically applied hoof treatment composition concentrate New aqueous concentrates adapted for dilution to form use compositions, and methods of preventing or treating hoof diseases with these use compositions are provided. The compositions and concentrates comprise (and preferably consist essentially of) a quaternary ammonium compound, an acid and a surfactant. Preferred quaternary ammonium compounds include those selected from the group consisting of alkyl dimethyl benzyl ammonium salts, alkyl dimethyl ethyl benzyl ammonium salts, dialkyl dimethyl ammonium salts, dialkyl methyl benzyl ammonium salts, and mixtures thereof. The inventive methods comprise diluting the concentrate to form a use composition and applying the use compositions to the affected areas by spraying, under a bandage, or in a footbath. The invention is particularly well-suited for treating papillomatous digital dermatitis.
CN101548971A Application of lignin flavanonol in preparation of antiviral drugs The invention relates to application of lignin flavanonol in preparation of antiviral drugs, particularly, the invention relates to a chemical compound as formula (I), (+-)-2-[2,3-dihydro-2-(3,5-dimethoxy-4-hydroxy phenyl)-3-hydroxymethyl-1,4-benzodioxane-5]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyrone-4-ketone, or use of its medicinal salt used for preparing drugs for repressing virus infection caused by herpes simplex virus HSV-1 and/or drugs for curing oral ulcer. The chemical compound is prepared by chemical synthesis, pharmacological experiments shows that, the chemical compound has powerful inhibitory action to the herpes simplex virus HSV-1, and the half inhibitory concentration value IC[50] is 39.41 mg/mL.
WO2012051204A3 Antimicrobial formulations that aid in wound healing The invention discloses compositions and formulations for the treatment of clean or infected wounds, some of the inventive formulations can be used to reduce or eliminate microbial contamination from surfaces such as skin, and inanimate objects such as countertops, cooking utensils, medical devices, cookware, food, grooming aids and agricultural biocides, and the like. Some of these compositions and formulations are well suited for use in wound dressings. Some of the formulation can kill and/or inhibit the growth of pathogenic bacteria, fungi, spores and viruses. The formulations comprise a compound such as an osmoticum in high enough concentration to create an osmotic gradient and at least one compound that acts to comprise the integrity of a microorganism's membrane or cell wall. These formulations may optimally include at least one agent that thickens the formulations. In some aspects the formulation is in the form of an emulsion.
US20060014242 Methods of modifying feeding behavior, compounds useful in such methods, and DNA encoding a hypothalamic atypical neuropeptide Y/peptide YY receptor (Y5) This invention provides methods of modifying feeding behavior, including increasing or decreasing food consumption, e.g., in connection with treating obesity, bulimia or anorexia. These methods involve administration of compounds are selective agonists or antagonists or the Y5 receptor. One such compound has the structure: In addition, this invention provides an isolated nucleic acid molecule encoding a Y5 receptor, an isolated Y5 receptor protein, vectors comprising an isolated nucleic acid molecule encoding a Y5 receptor, cells comprising such vectors, antibodies directed to the Y5 receptor, nucleic acid probes useful for detecting nucleic acid encoding Y5 receptors, antisense oligonucleotides complementary to any unique sequences of a nucleic acid molecule which encodes a Y5 receptor, and nonhuman transgenic animals which express DNA a normal or a mutant Y5 receptor.
US7179823 5-membered n-heterocyclic compounds with hypoglycemic and hypolipidemic activity A compound of formula (I) F wherein R1 represents a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; x represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: —CO—, —CS—, —CR4(OR5)— or —NR6— wherein each of R4 and R6 represents a hydrogen atom or a hydrocarbon group which may be stubstituted, R5 represents a hydrogen atom or a protective group for a hydroxyl group; m represents an integer of 0 to 3; Y represents an oxygen atom, a sulfur atom, or a group of the formula: —SO—, —SO2—, —NR7—, —CONR7— or —NR7CO— wherein R7 represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents an aromatic ring which may further have 1 to 3 substituents; n represents an integer of 1 to 8; ring B represents a nitrogen-containing 5-membered hetero ring which may further be substituted by an alkyl group.
CA2854946A1 Apricitabine and pi combination therapy The present invention provides a method of treating HIV-1 infection in a subject. The method comprises administering to the subject a combination of anti-HIV-1 agents wherein the combination comprises an effective dose of Apricitabine and an effective dose of Atazanavir.
US20100249069 S1p3 receptor inhibitors for treating pain Disclosed herein are compositions and methods for treating pain using S1P3 receptor inhibitors.
US20110117090 Adam-15 antibodies and immunogenic peptides The present invention relates to antibodies and antigen-binding fragments thereof, immunogenic peptide(s), and siRNA molecules which are capable of inhibiting neovascularization and/or angiogenesis and endothelial cell proliferation. The invention relates to antibodies and antigen-binding fragments thereof with specificity towards the metalloprotease domain of ADAM 15 and to immunogenic peptide(s) that elicits such antibodies. The invention also relates to compositions and kits comprising the antibodies and immunogenic peptide(s) of the invention, as well as methods and uses of the antibodies and antigen-binding fragments thereof and immunogenic peptide(s), as well as siRNA molecules.
WO2007069555A1 Novel 16-membered cyclic 4”-0-carbamoyl azalide derivative and process for producing same Disclosed is a compound represented by the general formula (1) below or a pharmaceutically acceptable salt thereof. Also disclosed are a process for producing such a compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition and antibacterial agent containing such a compound or a pharmaceutically acceptable salt thereof. (1) [In the formula, R1 represents a hydrogen atom or a C2-6 linear alkylcarbonyl group; R2 represents a hydrogen atom or a C2-6 alkylcarbonyl group; R3 represents a C1-6 alkyl group which may be substituted by a hydroxyl group or the like; R4 represents a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, an Ar-B- group (wherein Ar represents an aryl group or a heterocyclic group, and B represents a C1-6 alkyl group or a C2-6 alkenyl group) or the like; and R5 and R6 independently represent a hydrogen atom, a C1-6 alkyl group which may be substituted by a hydroxyl group, or a C2-6 alkenyl group.]
CN101716172B Application of miltipolone or pharmaceutically acceptable salts thereof in pharmacy The invention discloses an application of miltipolone or pharmaceutically acceptable salts thereof in the preparation of medicines for preventing or curing diseases related to Fe2+. A cancer cell inhibiting effect of the medicines prepared by the miltipolone or the pharmaceutically acceptable salts thereof realizes the purpose of anticancer through inhibiting cancer cell proliferation ; and particularly, the invention provides new choices of the medicines for curing or preventing human lung cancer, human liver cancer, human cervical carcinoma, human breast carcinoma, leukocythemia, fibrosarcoma, or gastric cancer.
US20120231047 Therapeutic agent delivery for the treatment of asthma via implantable and insertable medical devices Methods for the treatment of asthma are provided, which comprise: (a) providing an implantable or insertable medical device that comprises an asthma treatment agent; and (b) inserting or implanting the medical device within the lungs (e.g., the trachea or the bronchial tree) of a patient, whereupon the therapeutic agent is delivered to the patient in an amount effective to reduce or eliminate the symptoms of asthma. Also disclosed herein are medical devices and kits for carrying out such methods.
EP1082961B1 Sleep inducing agent comprising prostaglandin derivatives A sleep inducing agent comprising, as an active component, a prostaglandin derivative represented by formula (1), wherein X represents a halogen atom, Y represents a group represented by (CH2)m, a cis-vinylene group or a phenylene group, Z represents an ethylene group, a trans-vinylene group, OCH2 or S(O)nCH2, R<1> is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with a C1-4 alkyl group, a C4-13 cycloalkylalkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, an C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R<2> represents a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl, m is an integer of 1 to 3, and n is 0, 1 or 2, or a pharmaceutically acceptable salt or hydrate thereof.
CN1813781A Use of high-dose baicalin for preparing antivirus or antibacterial-anti-inflammatory drug The present invention relates to an application of large dose baicalin in the preparation of antiviral and antimicrobial inflammation-relieving medicine. The dose of baicalin application per day is 200-1000 mg. Its quality can be controlled, and its stability is good.
CN102631342A Application of epigallocatechin and pharmaceutical composition of epigallocatechin The invention discloses an application of epigallocatechin and a pharmaceutical composition of epigallocatechin. The epigallocatechin has obvious effect of reducing concentration of blood uric acid and can form a novel potential medicament used for treating hyperuricemia. In the medicament used for treating hyperuricemia, the epigallocatechin is taken as active ingredients used for treating the hyperuricemia, and the epigallocatechin is prepared into various officinal formulations by adopting a conventional method with pharmaceutically acceptable excipient and/or an officinal carrier together.
US6875767 (5-cyano-2-thiazolyl)amino-4-pyridine tyrosine kinase inhibitors The present invention relates to compounds having the formula I: which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions. The compounds of the present invention are useful in treating angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
CN103393651A Application of Sarcaboside B to preparation of medicament for treatment of chronic obstructive pulmonary disease The invention discloses application of Sarcaboside B to the preparation of medicaments for the prevention and treatment of chronic obstructive pulmonary diseases. The application of Sarcaboside B to preparation of medicaments for treatment of chronic obstructive pulmonary diseases involved in the invention is disclosed for the first time. As the Sarcaboside B has a novel skeleton type and unimaginably strong activity in inhibition of chronic obstructive pulmonary diseases, no other compound can give any enlightenment. The invention has outstanding substantive distinguishing features and makes substantial progress in treatment of chronic obstructive pulmonary diseases.
US20100316581 Skin External Preparations To provide skin external preparations characterized in that the initial permeation rate of oil-soluble drugs (e.g. retinol and tocopherol acetate) is controlled to achieve their sustained release to thereby reduce skin irritation and that they also possess a fresh feel while featuring high degrees of safety and stability. A skin external preparation which comprises a finely dispersed, oil-soluble drug containing wax composition, the composition containing a solid or semisolid wax, a nonionic surfactant, an aqueous dispersion medium, and an oil-soluble drug, the mass ratio of the nonionic surfactant to the wax being 1.0 or more, and the wax, with the oil-soluble drug contained therein, being finely dispersed in solid or semisolid form in the aqueous dispersion medium.
EP2070531A1 Pharmaceutical preparation containing histamine H2-receptor antagonists having wound healing activity at low doses The invention relates to a pharmaceutical preparation containing one or more histamine receptor antagonists at a concentration of less than 100 µg/mL for the topic treatment of dermatologic, vaginal, rectal, and ophthalmic wounds, abrasions, ulcerations, burns and sores.
CN1970056A Taste improved 'Xin Xue' powder Disclosed is a kind of flavoring granule for solving the problems of bad taste and bitterness, wherein screening tests of various dosage and proportion are conducted to a large quantity of flavoring agents, by adding albumen candy, the taste of the granule can be improved.
WO2012097478A1 Bicyclic carboxamide inhibitors of kinases The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X1, X2, X3, X4, R1, R2, R3, A, B, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
CN101724005A Novel anti-cancer purely natural medicine (11-carbonyl-beta-acetyl boswellic acid) The invention relates to a novel broad spectrum purely natural medicine that can specifically inhibit phosphorylation of protein T-kappa-B to prevent nuclear transport of T-kappa-B so as to inhibit the growth of cancer cell, thereby treating cancer. The novel medicine is a natural extractive, and has the advantages of low production cost, high curative effect and less side effect.
US20080146592 Method of Treating Preeclampsia Employing Metolazone A method of treating preeclampsia includes administering to a patient a therapeutically effective dose of metolazone. The dose is less than a diuretic dose. The treatment is effected without adverse on the fetus and without substantial volume reduction of intravascular extracellular fluid
WO2013084237A1 Deuterated tetramethyl dioic acids, compositions comprising them and uses thereof This invention relates to deuterated tetramethyl dioic acids, compositions comprising them and uses thereof in the treatment of Metabolic Syndrome and any diseases, disorders or symptoms associated therewith.
US20120294826 Methods, kits and compositions for ameliorating adverse effects associated with transfusion of aged red blood cells The present invention provides, inter alia, methods for ameliorating an adverse effect in a patient caused by an acute transfusion into the patient of a composition containing aged red blood cells using an iron chelator. Apparatuses and kits for ameliorating such adverse effects are also provided.
US20100261791 Compositions and Methods for Improving or Preserving Brain Function The present invention is related to mammalian nutrition and effects thereof in individuals with age associated cognitive decline such as Age Associated Memory Impairment (AAMI) or a dementing illness such as Alzheimer's disease or related dementia, or Mild Cognitive Impairment, such as improving performance in, or reversal, prevention, reducing and delaying decline in, one or more of cognitive function, memory, behavior, cerebrovascular function, motor function, and/or brain physiology are seen. In particular, the present invention utilizes medium chain triglycerides, in one embodiment, administered as part of a long-term treatment regimen, to preserve or improve learning, attention, motor performance, cerebrovascular function, social behavior, and to increase activity levels, particularly in aging mammals.
CN1602860A Dripping pills of clemastine fumarate and its preparation method The invention uses super micro shattering and drop pills producing the technology to produce fenfluramine drop pills, reaching the purposes such as increasing speed, and dissolution of disintegration, increasing the medicine stability, reducing the dose of auxiliary materials and decreasing cost, with rapid effect and convenient use. It can be buccal as well as deglutition, has remarkable conformity, and is especially suitable for children, older man, sicker in bed or with difficulty of swallowing.
CN101773510A Separation preparation of isovaleryl spiramycin III and application thereof The invention relates to the separation of antibiotics and the application thereof in resisting infectious diseases, in particular to a single-component compound of isovaleryl spiramycin III; rokitamycin samples are separated with a high performance liquid chromatography via sample crude separation, efficient purification, sample post-processing and the like so as to obtain the pure product of the isovaleryl spiramycin III compound; and biological test results indicate that the antibacterial activity of the component III compound is superior to that of rokitamycin and is obviously superior toa control group, which lays the foundation for developing clinically effective single-component antibiotics of the isovaleryl spiramycin III.
WO2010016931A2 Polymorphs of fluticasone furoate and process for preparation thereof Provided are polymorphs of fluticasone furoate and processes for preparation thereof.
WO2013178846A1 Pharmaceutical composition comprising diacetylmorphine and naloxone for oral administration The invention relates to a pharmaceutical composition comprising diacetylmorphine and naloxone for oral administration, comprising diacetylmorphine or one of the pharmaceutically acceptable salts thereof, naloxone or one of the pharmaceutically acceptable salts thereof and at least one pharmaceutically acceptable excipient, in which the weight ratio of diacetylmorphine:naloxone is between 24:1 and 26:1. The invention also relates to a tablet with the aforementioned composition and to the use of said composition or tablet for the preparation of a drug for the treatment of addiction to opioid substances.
US7307071 RAF-MEK-ERK pathway inhibitors to treat cancer Materials and methods for treating certain cancers are described, preferably cancers that result from the up-regulation of the RAF-MEK-ERK pathway, and more preferably chronic myelogenous leukemia, and which cancer is preferably resistant to the inhibition of the Bcr-Abl tyrosine kinase, imatinib.
CN103735532A Lutein ester microcapsule and preparation method thereof The invention discloses a lutein ester microcapsule, mainly comprising core material lutein ester powder, vegetable oil for dissolving the core material, a wall material, an antioxidant and an emulsifier, wherein the lutein ester microcapsule is prepared by the processes of preparing an oil-phase solution and a water-phase solution, and then mixing and emulsifying the oil-phase solution and the water-phase solution. No organic solvent is used in the overall process of preparation of the lutein ester microcapsule, the microcapsule wall material mainly is carbohydrate, and is wider in source and higher in safety, and the obtained lutein ester microcapsule is applicable to application in the fields such as a food and a medicine, and has high commercial value. In addition, the lutein ester microcapsule prepared by the method can be stably stored for a long period of time at room temperature, and has important significance on storage, transportation and use of the lutein ester.
CN101502506B Medical use of 3-(3,4-dihydroxyphenyl)-acrylic acid 2-(3,4-dihydroxyphenyl)-ethyl ester The invention discloses the application of caffeic acid 3,4-dihydroxy-phenethyl ester, prodrug or pharmaceutically acceptable salts thereof in the preparation of anti-tumor medicaments, the tumor is selected from digestive system tumors, lung cancer, mammary cancer, ovarian cancer, prostatic cancer, central nervous system tumors, melanoma or leukemia, wherein, the digestive system tumor particularly represents gastric cancer, colon cancer, liver cancer or pancreatic cancer tumors.
US20080102066 Ultrapure transferrin for pharmaceutical compositions The present invention relates to an ultrapure human transferrin, and to methods for manufacturing the ultrapure transferrin. The transferrin may be holo-, apo- or at any desired degree of iron saturation. The invention further relates to the use of ultrapure transferrin as the protein moiety of conjugates, and to pharmaceutical compositions comprising ultra transferrin alone as well as in the form of a conjugate.
US20130023538 Heteroaryl Derivatives as CFTR Modulators The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
EP2516404A2 Preparation of bendamustine and its salts The present application relate to processes for the preparation of bendamustine and its pharmaceutically acceptable salts.
US7049124 Hyaluronidase from the Hirudinaria manillensis isolation, purification and recombinant method of production The present invention relates to the isolation, purification and characterization of a hyaluronidase which derives from the tropical leech Hirudinaria manillensis. Therefore, according to this invention, the enzyme was called “manillase”. The invention is furthermore concerned with the recombinant method of production of manillase which includes the disclosure of DNA and amino acid sequences as well as of expression vectors and host systems. Finally, the invention relates to the use of manillase for therapeutic purposes, for example, for the treatment of myocardial diseases, thrombotic events and tumors.
CN101138556A Terbinafine or its salt film forming gel composition and uses thereof The present invention discloses a compound of an Terbinafine or the halo-Terbinafine membrane forming gel, which comprises the components of the following weight percentages comprising 0.5 percentage to 7 percentage of alkyl cellulose, 1 percentage to 10 percentage of etherifying agent, 0.5 percentage to 5 percentage of cross linking agent, 0.5 percentage to 5 percentage of accentuator, 75 percentage to 90 percentage of dissolvant0.1 percentage to 5 percentage, of Terbinafine or the halo-Terbinafine. The cross linking agent is the saturated fat or the alcoholic acid, the chemical general formula of which is CnH2n+2-m-l(OH)m(COOH)l. Among the formula, m or n or 1 is the integer and the n is no less than m, which is no less than 2. 1 is no less than 0 and the result of m plus 1 is 4 to 8. The result of n plus 1 is 4 to 8. In the present invention, the compound of the Terbinafine or the halo-Terbinafine local membrane forming gel is applied for treatment of the local fungus inflammation. A water drain protective membrane with smooth property, firm property, wear-resisting property and duration property is formed on the surface of the ulcer when the present invention is applied. Compared with all kinds of formulations of the Terbinafine or the halo-Terbinafine in the present technique, the membrane formed by the gel compound is not likely to experience fracture, dissolution or corrosion. The membrane has the properties of long maintenance time and slow releasing of the medicine.
WO2014048071A1 Method and pharmaceutical composition for inhibiting pi3k/akt/mtor signal path The present invention relates to a pharmaceutical composition of PRCP antagonist, PREP antagonist, or PRCP-PREP dual antagonist. The present invention also relates to a pharmaceutical composition jointly using PRCP antagonist and mTOR antagonist, or jointly using PREP antagonist and mTOR antagonist, or jointly using PRCP-PREP dual antagonist and mTOR antagonist. In addition, the present invention also relates to a method for utilizing the pharmaceutical compositions to treat and prevent cancers and diseases related to insulin receptor substrate protein and PI3K/AKT/mTOR signal pathway.
US20100179104 Synthetic nutritional formulations The present invention provides a synthetic nutritional formulation comprising a substantially pure free N-acetyl glucosamine in concentrations effective for enhancing organ development, enhancing an immune response, or increasing tissue repair or healing in a subject. A synthetic nutritional formulation of the invention may optionally comprise one or both of substantially pure free sialic acid and/or substantially pure free fucose.
CN103271895A Stable calcium dobesilate containing pharmaceutical composition and preparation method thereof The invention overcomes the defect in the prior art and provides a stable calcium dobesilate containing pharmaceutical composition, and the composition is added with magnesium oxide, calcium oxide and other drying protection components, and can absorb water content in environment and protect main drug from being in a high moisture state. The invention provides a pelletizing method by waterless ethanol and other non-aqueous solvents, and the prescription is added with correspondingly acceptable carrier or excipient and other pharmaceutic adjuvants for preparing common tablet, film coated tablet, capsule, sustained release tablet or capsule. Compared with the prior art, the medicament stability is obviously improved, and the validity and security are guaranteed.
CN103520109A Preparation method of puerarin solid dispersing agent The invention discloses a preparation method of a puerarin solid dispersing agent. The method is carried out according to the following steps of: mixing puerarin and a solid-phase reagent, then placing into a ball mill, and carrying out ball milling till the puerarin and the solid-phase reagent are uniformly mixed; taking out ball-milled powder, and screening to obtain the puerarin solid dispersing agent, wherein the solid-phase reagent is one or a mixture of more than two of calcium carbonate, calcium bicarbonate, zinc carbonate, magnesium carbonate, magnesium bicarbonate, zinc acetate and calcium acetate, and the mass ratio of the puerarin to the solid-phase reagent is 1:(0.1-10). According to the invention, a crude medicine is uniformly dispersed into a solid-phase carrier in the form of ultra-fine crystals by utilizing mechanochemical effect and is interacted with the solid-phase carrier through a hydrogen bond, van der waals force, and the like, so that the solubility, dissolution rate and oral bioavailability of the medicine are enhanced.
US7132420 Aspartic protease inhibitors The present invention provides an aspartic proteinase-inhibiting compound of the formula: wherein a, b, c, d, and e, can be the same or different and each are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen, wherein R7 and R8 are independently H or an alkyl. Substituents R1 or R2 are each H or an alkyl. Substituent R3 is a straight chain or branched alkyl, alkenyl, or alkynyl substituent, or is a cycloalkyl. Substituent A is OH, NH2, or SH. Further provided are pharmaceutical compositions, which include a therapeutically effective amount of at least one of the foregoing compounds, and therapeutic methods of using the foregoing compounds.
US20100303716 Switchable nano-vehicle delivery systems, and methods for making and using them The invention provides nanodevices or products of manufacture for use as drug delivery vehicles. In one aspect, the invention provides nanodevices or products of manufacture having on-off release mechanisms, e.g., that are “switchable”, or “actuatable” (for example magnetically or ultrasonically switchable), for compounds contained within, e.g., for use as drug delivery nano-vehicles having on-off drug release mechanisms, and their therapeutic applications.
US20090170871 IL-8 Receptor Antagonists This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
CA2130787C Ursodeoxycholic acid-containing medicament in a liquid administration form The active agent ursodeoxycholic acid has proved therapeutically active in infants, inter alia for the treatment of cholestatic hepatic diseases. A problem when administering this active agent, a bile acid, to infants is its extreme bitterness. As a result of the present invention a taste-acceptable, liquid administration form for ursodeoxycholic acid with an adequately high active agent concentration is described. The liquid to be ingested is a suspension prepared accompanied by the addition of a swelling and/or thickening agent, which contains the active agent mainly in fine crystalline form as the disperse phase and only in a much smaller proportion dissolved in the aqueous dispersant. A remaining residual bitterness can be additionally masked by the addition of .beta. -cyclodextrin or suitable taste correcting agents.
WO2008110863A1 Indazole derivatives and their use as vanilloid receptor ligands The present invention relates to indazole derivatives of the following formula I, which can be used as vanilloid receptor ligands, processes for their preparation, and their use in treating diseases, conditions and/or disorders modulated by vanilloid receptors. (I)
EP1921136A1 Nucleic acid for treatment or prevention of immunodeficiency virus infection A nucleic acid comprising a transcription regulation sequence whose transcription is induced by a trans-acting factor of a human immunodeficiency virus and a gene encoding a polypeptide having an endoribonuclease activity specific to single-stranded RNA, wherein the gene is located in such a position that the expression of the gene can be regulated by the transcription regulation sequence; a method for production of a cell showing an inhibited replication of a human immunodeficiency virus therein, the method comprising the step of introducing the nucleic acid into a cell; and a method for treatment or prevention of a human immunodeficiency virus infection.
CN1900076A Tetrahydro proto-berberine compounds, and their preparing method and use The present invention provides tetrahydro protoberberine compounds as shown and their pharmaceutically acceptable salts. These compounds have activity on dopamine acceptor, and thus may be used in treatment, especially treatment on schizophrenia. The present invention also provides their preparation process.
US20080014252 Topical compositions with long lasting effect Topical pharmaceutical formulations and compositions for transdermal delivery of a variety of active agents are described. The formulations and compositions are formulated to provide a long lasting effect of the agent being delivered. The formulations and compositions of the present invention contain a transdermal vehicle and an adrenergic drug. The formulations and compositions may also contain guaifenesin.
EP1785134A2 Thiazole, imidazole and oxazole compounds and treatments of disorders associated with protein aging Use of a compound of formula I or IA below in the manufacture of a medicament for use in treating (i) diabetes, treating or ameliorating (ii) adverse sequelae of diabetes, (iii) kidney damage, (iv) damage to blood vasculature, atherosclerosis, peripheral vascular disease, coronary heart disease or heart failure, (v) hypertension, (vi) retinopathy, (vii) peripheral neuropathy, (viii) cataracts, (ix) osteoarthritis, (x) rheumatoid arthritis, (xi) Alzheimer's disease, (xii) damage to a tissue caused by contact with elevated levels of reducing sugars or (xiii) stroke, (xiv) improving the elasticity or reducing wrinkles of the skin of an animal or (xv) increasing RBC deformability: wherein: a. J is oxygen, sulfur or N-Rd, b. the bond between carbons 4 and 5 is a single bond or a double bond; c. Ra and Rb are: 1. independently selected from alkyl and cycloalkyl; or 2. together with their ring carbons form a C5-C7 fused cycloalkyl ring having up to two double bonds including a fused double bond of the containing group, which cycloalkyl ring can be substituted by one or more of alkyl and fluoro; d. Rc is alkyl; and e. Rd is alkyl or hydrogen; or a pharmaceutically acceptable salt of said compound.
US8703729 Mixture comprising an inhibitor or suppressor of a gene and a molecule binding to an expression product of that gene A mixture comprising at least one inhibitor or suppressor of the expression of a gene and at least one molecule binding to an expression product of said gene.
US20110301125 Method for Treating Macular Degeneration Provided herein are novel and useful methods for preventing, treating, or ameliorating a macular degeneration such as dry macular degeneration, wet macular degeneration and age related macular degeneration in a patient.
WO2007069744A1 Composition for prevention/amelioration of metabolic syndrome The object is to provide a composition (pharmaceutical, food) which is effective for the prevention/amelioration of metabolic syndrome, the prevention/amelioration of the decreased blood HDL cholesterol level and the prevention/amelioration of hyperinsulinism, dyslipidemia, fatty liver, hyperlipemia or arteriosclerosis and is highly safe, and to provide an effective and safe agent for improving the expression of a gene involved in lipid metabolism. Disclosed is a composition for the prevention/amelioration of metabolic syndrome, a composition for the prevention/amelioration of the decreased blood HDL cholesterol level, or an anti- hyperinsulinism, anti-dyslipidemia, anti-hyperlipemia, anti-fatty liver or anti-arteriosclerosis composition, which comprises three branched amino acids isoleucine, leucine and valine as active ingredients. Also disclosed is an agent for improving the expression of a gene involved in lipid metabolism, comprising three branched amino acids isoleucine, leucine and valine as active ingredients.
CN103169677A Adefovir dipivoxil tablet for treating hepatitis B and preparation method thereof The invention discloses an adefovir dipivoxil tablet for treating hepatitis B and a preparation method thereof, and belongs to the technical field of medicines, wherein each 1000 adefovir dipivoxil tablets are prepared from the following materials by weight: 10g of adefovir dipivoxil (AD), 70g of milk sugar, 30g of microcrystalline cellulose, 9g of sodium carboxymethyl starch, 1g of gum acacia and 0.5g of magnesium stearate. The adefovir dipivoxil tablet disclosed by the invention is a drug which is low in price, has no cross resistance for treating the hepatitis B, and has the advantages of inbibitional effects on a mutant virus strain with resistance to lamivudine.
US20100286227 Compounds from Mycelium of Antrodia Cinnamomea and Use Thereof The present invention relates to compounds from mycelium of Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) infection.
CN103599449A Liuwei Anxiao pharmaceutical composition and application of preparation thereof in preparation of drug for treating alcoholic hepatitis The invention discloses a Liuwei Anxiao pharmaceutical composition and application of a preparation thereof in preparation of a drug for treating alcoholic hepatitis. The Liuwei Anxiao pharmaceutical composition comprises six medicine ingredients, namely, Tibet inula root, rheum officinale, rhizoma kaempferiae, fumed gypsum, fructus chebulae and tronae. The clinical test shows that the Liuwei Anxiao pharmaceutical composition can protect alcoholic liver injury and can also obviously improve AST (Aspartate Transaminase), ALT (Alanine Aminotransferase), GGT (Gamma Glutamyl Transpeptidase), TBiL (Total Bilirubin) and other biochemical indexes.
CN102302447A Novel taxol lipid microsphere injection and preparation method thereof The invention discloses a novel taxol lipid microsphere injection containing amphiphilic polyamino acid and a preparation method thereof. The injection contains taxol, amphiphilic polyamino acid, oil for injection, an emulsifying agent, an auxiliary emulsifying agent, a potential regulator, an antioxidant, a metal chelating agent, an iso-osmotic adjusting agent and water for injection, wherein the amphiphilic polyamino acid is a segmented copolymer consisting of a hydrophilic chain segment and racemic hydrophobic polyamino acid. The novel taxol lipid microsphere injection represents a microscopic structure different from that of a traditional lipid microsphere preparation, therefore the injection has excellent stability superior to that of the traditional lipid microsphere preparation. Inthe preparation, polyoxyethylene castor oil is not contained, VE (vitamin E) is not used massively, and no organic solvent is introduced; in addition, the injection can tolerate thermal pressure sterilization, has the advantages of no irritation, low toxicity, good stability and low cost, and is suitable for industrial production in large scale.
CN101244082A Animal bone calcium and preparation thereof The invention relates to the preparation of animal bone calcium the main material of which is animal bone, belonging to health food field. The technical proposal is to provide a bone calcium which has good water-solubility. The invention is characterized in that the components are: total phosphorus calculated as P is 1.8 to 2.0%; calcium is 15 to 16%. The preparation method is: the enzymolysis liquid and the enzyme dissolved yak bone are obtained after the animal bone is cleaned, immersed, heated and enzyme dissolved; the dried zymolyte is obtained after the enzymolysis is degreased, filtered, and dried; the enzyme dissolved yak bone is dried and ground after being degreased; the dried zymolyte and ground animal bone is mixed in any proportion to get the bone calcium. The animal bone calcium has the advantages that the water-solubility is good; the absorption to human body is good; the calcium contents are high; the content of a plurality of amino acid which is necessary to human body is rich. In a word, the invention provides a new calcium supplement product and the preparation method. The popularization and application of the product is good for changing the calcium deficiency condition of human beings, in particular to Chinese and improving the health condition of human beings.
WO2008065100A1 Substituted estratrien derivatives as 17beta hsd inhibitors This invention relates to novel substituted estratrien derivatives of general formula (I) useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17- HSD) type 1, type 2 and/or type 3 enzyme, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds.
WO2012029348A1 Granules containing bitter drug and orally disintegrating tablet The objective of the present invention is to provide a bitter-drug-containing powdered medicine or granular medicine and an orally disintegrating tablet that achieve both suppression of bitterness in the oral cavity and superior dissolution in the stomach. The drug-containing granules, which comprise (a) core particles containing the bitter drug and (b) a masking coating film that coats the core particles, are characterized by the masking coating film containing at least one excipient selected from D-mannitol, lactose, trehalose, xylitol, maltitol, and erythritol, and at least one polymer selected from a methacrylate copolymer (S), a methacrylate copolymer (L), a methacrylate/ethyl acrylate copolymer, an ethyl acrylate/methyl methacrylate copolymer, or the like.
WO2006129594A1 Method for producing nucleic acid-containing complex preparation It is intended to provide a method for producing a nucleic acid-containing complex preparation which can be subjected to filter sterilization and administered intravenously to human and in which the stability of a polynucleotide contained in the nucleic acid-containing complex preparation is maintained. The invention relates to the method for producing a nucleic acid-containing complex preparation characterized by mixing a solution in which two polynucleotides which can form a double strand (for example polyI and polyC) in a single stranded form are contained in the same solution and a cationic carrier or a raw material solution before forming a cationic carrier and subjecting the mixture to a dispersion treatment.
CN101744803A Method for preparing oridonin solid dispersion The invention discloses a method for preparing oridonin solid dispersion, comprising the following steps: evenly mixing oridonin with auxiliary according to the mass ratio of 1:4 to 1:10, putting the mixture into an autoclave and then sealing the autoclave, wherein the auxiliary is polyvinylpyrrolidone PVP K17; placing the autoclave in ice-water bath for cooling and feeding CO2 into the autoclave; placing the autoclave in water bath at 55 to 60 DEG C, implementing static reaction for 12 to 24 hours after the autoclave reaches 55 DEG C and 8-14MPa for 10 to 15 minutes, rapidly decompressing and collecting reaction products in the autoclave. The oridonin solid dispersion prepared according to the method, compared with physical mixture thereof, is increased in AUC value, which shows that the oridonin solid dispersion has obvious absorption promoting effect for oridonin.
WO2012032185A1 Method for producing crystalline 5-aminosalicylic acid The invention relates to a method for producing crystalline 5-aminosalicylic acid with a particularly high tap and/or bulk density.
CN101693050A Composition containing clerodendranthus spicatus aqueous extract The invention discloses a composition containing a clerodendranthus spicatus aqueous extract, which comprises the clerodendranthus spicatus aqueous extract and hydrochlorothiazide, wherein the weight ratio of the clerodendranthus spicatus aqueous extract and the hydrochlorothiazide which have the weight being equivalent to 1 gram of primary medicine is 1:0.005-0.01. Compared with the prior art, the invention has the advantages that the water-soluble beneficial components packaged in cellulose can be sufficiently extracted by using composite cellulase to dissolve the cellulose in clerodendranthus spicatus stalks in the extracting process of the clerodendranthus spicatus aqueous extract and simultaneously the litholytic and diuretic functions of the clerodendranthus spicatus aqueous extract are enhanced by using the hydrochlorothiazide.
EP1782818A1 Pharmaceutical composition comprising lactobacilli and symethicone for the treatment of gastrointestinal pathologies A pharmaceutical composition comprising lactobacilli such as Lactobacillus Sporogenes and symethicone that can be used for the treatment of the pathologies of the gastrointestinal apparatus, in particular in children and nurslings.
WO2006129134A1 Synergic combinations comprising a styrylquinoline compound and other hiv infection therapeutic agents The invention relates to a combination comprising a quinoline compound or its salt, according to general formula (I) and at least one HIV infection therapeutic agent selected from the group consisting of entry inhibitors, reverse-transcriptase inhibitors, strand-transfer inhibitors, protease inhibitors, and maturation inhibitors. Said combination has therapeutic synergy in the treatment of an HIV infection compared with the quinoline compound, or HIV infection therapeutic agent alone.
WO2014036426A1 N-(3-fluorobenzyl)-2-(5-(4-morpholinophenyl)pyridin-2-yl) acetamide as protein|tyrosine kinase modulators The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention also relats to substantially pure compound 1 and substantially pure compound 1 salt (e.g., compound 1 hydrochloride salt and compound 1 benzenesulfonate salt). The invention further relates to methods of preparing substantially pure compound 1 and compound 1 salts.
WO2014102497A1 Dermatological composition comprising a pde7 inhibitor in a solubilised form, production method thereof, and use of same The invention relates to anhydrous compositions comprising at least one PDE7 inhibitor and at least one specific organic solvent.
CN101745116A Preparation method for copper ion chelate adsorbing medium used for curing Wilson's disease) The invention relates to a preparation method for copper ion chelate adsorbing medium used for curing Wilson's disease) in blood purification therapy, which obtains the copper ion chelate adsorbing medium by further bonding a copper ion sorbitol trine or tetraethylpentam through an ring-opening reaction between the epoxide groups on a polymer microsphere. The preparation method is simple to be operated, is easy to be realized and has a low preparation cost. The immobilized trine or tetraethylpentam adsorbing medium obtained through preparation has quick absorbing characteristic (reaching absorbing balance in 0.5 hour) and ideal absorbing effect (the absorbing amount can reach 80.4 plus or minus 2.8mg of copper ion/g of absorbing medium) to the copper ions. The immobilized trine or tetraethylpentam adsorbing medium obtained through the preparation method has excellent application prospect in curing Wilson's disease.
EP0799034B1 Use of aromatic or branched chain amino acids for the treatment of movement disorders The present invention relates to a method of remitting or attenuating the symptoms of movement disorders which can be secondary to treatment of psychiatric disorders with antipsychotic drugs mainly neuroleptics, movement disorders that arise secondary to non-neuroleptic drugs in the treating of non-psychiatric disorders or primary neurological disorders. This treatment involves administering a meal enriched with large neutral amino acids or a dietary supplement of large neutral amino acids to patients suffering from these disorders.
CN1919173A Nimustine slow release injection for treating extracranial noumenal tumour Disclosed is a Nimustine slow release injection for treating extracranial solid tumours, which comprises effective anticancer dose of Nimustine or the combination of Nimustine and its synergists (such as 5-FU, cisplatin or 06-benzyl guanine). The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved.
CN1663568A Compound formulation for effectively preventing and treating virus infection The content of this invention is to present one kind of compound preparation, which comprises ganciclovir and glycyrrhizin, and the form can be oral taking, injection, external preparation. This compound preparation can be used to disease brought all kinds viral infection from clinic, and can also be used to curing inflammation, enhancing immunity function. The compound preparation comprises a variety of active factors with dose cured effectively, wherein dose rate of ganciclovir and glycyrrhizin varieties accordingly. For optimizationú¼the value of weight rate of medicinalable salt for ganciclovir and glycyrrhizin varieties 1:20 ~ 20:1 and optimized value is 1:5~5:1.
CN103349688A Bone disease treatment medicine The invention relates to a bone disease treatment medicine. The medicine is composed of an external ointment and an oral medicinal liquor which are cooperatively used, wherein the ointment is prepared through using 13-18 parts by weight of Panax Notoginseng saponin, 8-12 parts by weight of Radix Astragali, 24-27 parts by weight of Rhizoma Coptidis, 8-12 parts by weight of Sophora flavescens, 8-12 parts by weight of calcium carbonate, 14-17 parts by weight of hydrated silica, 8-12 parts by weight of calcium phosphate, and 4-7 parts by weight of an aqueous solution obtained after dipping medicines in water; and the medicinal liquor is prepared through using formula raw materials and a 43-60DEG liquor having a weight 3-5 times the formula raw materials, and the formula raw materials comprise 4-7 parts by weight of Rhizoma Coptidis, 3-7 parts by weight of Herba Cynomorii and 86-93 parts by weight of Polygonatum sibiricum. The ointment is used through external application, and has the characteristics of disinfection, sterilization, blood circulation promoting, blood stasis removal, blood viscosity reduction, use convenience and fast effectiveness. The medicinal liquor and the ointment complement each other in effects, so the synergistic effect, substantial effectiveness, and exterior and foundation strengthening are realized.
US20110263563 Ansamycin Hydroquinone Compositions Aspects of the present invention provide compositions comprising a sulfur containing compound and a compound of the formula (I); and also provide methods of their preparation and use.
US20060166255 Methods of using 48149, a human Aminopeptidase family member Isolated nucleic acids molecules, designated 48149 nucleic acid molecules, which encode human Aminopeptidase N, are disclosed. The invention provides methods of modulating 48149 activity, which is associated with the formation of atherosclerotic lesions in blood vessels. The invention further provides methods of treating, preventing and diagnosing cardiovascular disorders such as atherosclerosis, as well as disorders associated with the metabolism of lipids, for example, in the liver.
CN101125196A External applied medicine for treating lumbar vertebra, cervical vertebra and osteoarthrilis The present invention relates to an externally applied drug for the treatment of lumbar, cervical and bone joint diseases, which is characterized in that the present invention is prepared by the pharmaceutical raw materials with the following mix ratio by weight: 25 to 35 parts of Szechuan lovage rhizome, 20 to 30 parts of Chinese angelica, 35 to 45 parts of peach seed, 20 to 30 parts of safflower, 15 to 25 parts of sappan wood, 15 to 25 parts of cape jasmine fruit, 15 to 25 parts of nutgrass galingale rhizome, 15 to 25 parts of pangolin scales, 30 to 40 parts of leech, 1 to 3 parts of musk, 25 to 35 parts of dragon's blood, 20 to 30 parts of frankincense, 20 to 30 parts of myrrh, 15 to 25 parts of trogopterus dung, 15 to 25 parts of incised notopterygium rhizome, 15 to 25 parts of doubleteeth pubescent angilica root, 20 to 30 parts of pedate pinallia jackinthepulpit rhizome, 25 to 35 parts of scorpion, 15 to 25 parts of manchurian wildginger, 30 to 40 parts of dahurian angelica root, 25 to 35 parts of divaricate saposhnikovia root, 15 to 25 parts of great burdock achene, 20 to 30 parts of dried ginger, 25 to 35 parts of kusnezoff monkshood root, 25 to 35 parts of common monkshood mother root, 15 to 25 parts of pine nodular branch, 15 to 25 parts of siberian cocklour fruit, 20 to 30 parts of snake slough, 20 to 30 parts of tall gastrodia tuber, 30 to 40 parts of realgar, 35 to 45 parts of common floweringquince fruit, 15 to 25 parts of seaweed, 15 to 25 parts of kelp, 20 to 30 parts of lilac daphne flower bud, 20 to 30 parts of Peking euphorbia root, 25 to 35 parts of cochinchina momordica seed, 25 to 35 parts of Gleditsia sinensis stings, 25 to 35 parts of ephedra herb, 55 to 65 parts of hydrargyri oxydum rubrum, 10 to 20 parts of borax and 10 to 20 parts of borneol.
CN1864672A A solid dispersion of ambroxol hydrochloride and composition thereof The present invention relates to one kind of ambroxol hydrochloride dispersion and its preparation process and medicine composition. The ambroxol hydrochloride dispersion contains ambroxol hydrochloride and carrier material in the weight ratio of 1 to 0.3-10. The present invention aims at masking the bad smell of ambroxol hydrochloride.
CN103565747A Esomeprazole composition and preparation method thereof The invention provides an esomeprazole composition and powder injection prepared from the composition. The esomeprazole composition consists of esomeprazole or pharmaceutically acceptable salt or solvate thereof, a pH regulating agent, ethanol and tert butyl alcohol. The esomeprazole composition uses the ethanol and the tert butyl alcohol as solvents, regulates pH value of the solvent through a sodium hydroxide solution, dissolves an active ingredient, and prepares a stable preparation through a low-temperature freeze-drying method; and the esomeprazole composition is low in accessory amount and high in stability.
CN101385699A Sustained-released injection containing nitrosourea medicine A sustained release injection containing a nitrosourea drug consists of sustained release microspheres and a dissolvent, wherein, the sustained release microspheres comprise a nitrosourea drug selected from nimustine, carmustine and the like and/or an anticancer active component of topoisomerase inhibitor and a sustained release adjuvant, and the dissolvent is a common dissolvent or a special dissolvent containing a suspending agent. The suspending agent has the viscosity of 100cp-3000cp (at the temperature of 20-30 DEG C) and is selected from sodium carboxymethyl cellulose and the like; the sustained release adjuvant is selected from copolymer of polyphosphate esters p(LAEG-EOP) or p(DAPG-EOP) and the like, or copolymer or polyblend of the polyphosphate esters and PLA, polifeprosan, PLGA and poly(erucic acid dimmer-sebacic acid); the topoisomerase inhibitor is selected from camptothecin, hydroxyl camptothecin, topotecan, lurtotecanthe, irinotecan, etoposide or teniposide; the anticancer composite is also made into a sustained release implant, and injected into or placed inside or at the periphery of tumor to keep the effective drug concentration more than 60 days. The sustained release injection can also obviously reduce the general reaction of the drug, and selectively enhance the curative effects of non-operative therapies such as radiotherapy, chemotherapy and the like.
US20120259014 Topical retnoid solutions The present invention relates to a topical solution comprising a retinoid or its pharmaceutically acceptable salts thereof and a process of preparing it.
CN102050717A Dysideavillosa element A, element B and element C as well as preparation method and application thereof in preparation of drugs The invention relates to the technical field of medicine, in particular to sesquiterpene anthraquinone compounds of dysideavillosa element A, element B and element C, which are extracted from dysideavillosa as well as a preparation method and application thereof in the preparation of drugs. The structural formulas of the dysideavillosa element A, the element B and the element C are shown in the specification. The compounds can be used as protein tyrosine phosphatase 1B (PTP1B) inhibitors and insulin sensitizers through biological activity testing and be used for preparing drugs for treating type II diabetes, obesity and complications of type II diabetes and obesity.
EP1509519A1 Crystalline fluoroquinolone arginine salt form The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.
EP1740192B1 Cyclic dinucleotide for stimulating the immune of inflammatory response Cycic di-GMP, or a cyclic dinucleotide analogue thereof that has the same effect as cyclic di-GMP, stimulates or enhances immune or inflammatory response in a patient or enhances the immune response to a vaccine by serving as an adjuvant. Cyclic di-GMP, or a cyclic dinucleotide analogue thereof, also has neuroprotective properties for use as a neuroprotective agent to inhibit, treat, or ameliorate the effects of injuries, diseases, disorders or conditions that result in neurodegeneration.
US6884795 Pharmaceutical compositions and uses for androst-5-ene-3β, 17β-diol Androst-5-ene-3β,17β diol is used to treat or reduce the likelihood of acquiring osteoporosis or menopausal symptoms, or other diseases affected by estrogen receptor activity, and for conditions which respond well to DHEA treatment, but where a higher ratio of estrogenic to androgenic effects is desired. Combination therapies are included, as are kits and pharmaceutical compositions for providing the active ingredients of claimed methods and combinations.
US20080026079 Calcium aluminosilicate pharmaceutical A composition and method of treating symptoms of diarrhea that utilize administering an effective amount of an isolated calcium aluminosilicate anti-diarrheal (“CASAD”), wherein the isolated CASAD is substantially free from T4-dioxin and toxic heavy metal contamination, waiting a period of time; and repeating the administration of the composition until the symptoms of diarrhea are mitigated. The symptoms of diarrhea may be associated with chronic or infectious diseases, inflammatory proteins, treatment using drugs, or treatment using a chemotheraputic agent in a subject in need of treatment. The isolated CASAD is capable of binding inflammatory proteins, drug metabolites, and chemotherapeutic agents. The isolated CASAD can be administered in any suitable form, such as in tablet, powder, or suspension form, and can be administered by any suitable route, such as orally.
EP1244617B1 Substituted aminoalkylamide derivatives as antagonists of follicle stimulating hormone The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.
US8163734 Use of a mast cell activation or degranulation blocking agent in the manufacture of a medicament for the treatment of a patient subjected to thrombolyses The invention concerns the use of a mast cell activation- or degranulation-blocking agent in the manufacture of a medicament for preventing and treating cerebral complications caused by thrombolytic treatment. The invention also relates to treatment of patients suffering from cerebral complications associated with thrombolysis. Further, the invention provides thrombolytic compositions comprising a mast cell degranulation-blocking and/or mast cell activation-blocking agent present in a therapeutically effective amount to prevent or reduce any cerebral complications caused by the active thrombolytic component.
US20110064652 Nanoparticles for targeted delivery of active agents to the lung The present invention concerns a delivery system administered to the lung preferably by inhalation comprising a polymer-based nanoparticle; and a linker comprising a first portion non-covalently anchored to said nanoparticle, wherein at least part of said first portion comprises a hydrophobic/lipophilic segment embedded in said nanoparticle; and a second portion comprising a coupling group, preferably a maleimide compound, exposed at the outer surface of said nanoparticle. In accordance with one embodiment, the delivery system comprises one or more targeting agents, each covalently bound to said coupling group, preferably maleimide compound, and is administered as an aerosol in the therapy or diagnosis of lung cancer or bronchial dysplasia. In accordance with yet another embodiment, the delivery system comprises a drug and/or a radiopharmaceutical and/or a contrasting agent. A specific example for a linker in accordance with the invention is octadecyl-4-(maleimideomethyl)cyclohexane-carboxylic amide (OMCCA).
US7201914 May contain a viricide, a bactericide or bacteriostate, and/or an antiinflammatory agent; uses include control of microbial growth on gloved hands New medicaments and compositions having an antiperspirant agent and an antimicrobial agent, and methods based thereof, for control, prevention, amelioration, or treatment of perspiration and topical microbial contamination or infection of skin of the hands, feet, groin, face and other areas of the body, along with reduction or control of symptoms and side effects of such perspiration and microbial contamination or infection, are disclosed. Such medicaments and compositions can be used for various cosmetic, medicinal or pharmaceutical purposes, including control of microbial growth on gloved hands, control of microbial contamination of hands, control of chronic irritation or infection of hands, feet, groin, head, or other areas of skin associated with athletic participation, control of facial acne or other similar conditions, as a cosmetic foundation, or for control of foot odor or excessive foot perspiration.
US20100184729 New Pharmaceutical Compositions for Treatment of Thrombosis The present invention relates to novel pharmaceutical compositions comprising at least one direct thrombin inhibitor and at least one additional active compound selected from the groups consisting of platelet inhibitors, low molecular weight heparins (LMWH) and heparinoids as well as unfractionated heparin, factor Xa inhibitors, combined thrombin/factor Xa inhibitors, fibrinogen receptor antagonists (glycolprotein IIb/IIa antagonists) and Vitamin K antagonists, optionally together with one or more pharmaceutically acceptable excipients or carriers for the treatment of thrombosis.
US20110034381 Methods for Therapeutic Treatment of Benign Prostatic Hypertrophy (BPH) Therapeutic methods for treatment of benign prostatic hypertrophy by inhibition of the activity of insulin-like growth factor-I (IGF-I). Methods encompass the use of IGF-I antagonists, as well as the use of compounds that lower the effective level of IGF-I or interfere with post receptor effects of IGF-I action in the prostate.
US20110065673 Novel leukotriene receptor agonist It is an object of the present invention to provide a leukotriene receptor antagonist that can be conveniently prepared from a natural source. The object has been achieved by finding that a marine product such as a squid phospholipid extract or an Akiami paste shrimp phospholipid extract contains the antagonists of BLT and CysLT1, which are leukotriene receptors. Therefore, the present invention provides a dietary composition and a pharmaceutical composition for inhibiting the activity of leukotriene receptors, containing a squid phospholipid extract or an Akiami paste shrimp phospholipid extract.
CN103687597A PARP inhibitors for the treatment of CIPN The present invention relates to the method of treating chemotherapy-induced neuropathy in a subject in need thereof with the use of a poly(ADP-ribose)polymerase (PARP) inhibitor.
EP1299100B1 Method of treating hot flashes, using tachykinin receptor antagonist The present invention relates to methods of treating hot flashes and symptoms of hormonal variation in a patient, which methods include providing a tachykinin receptor antagonist and administering the tachykinin receptor antagonist to a patient experiencing a symptom of hormonal variation under conditions effective to treat the symptom of hormonal variation, which symptoms of hormonal variation can include hot flashes.
EP1232171B1 Method of preparing clarithromycin Clarithromycin can be easily prepared by reacting erythromycin A N-oxide with a methylating agent to obtain 6-O-methylerythromycin A N-oxide; and treating 6-O-methylerythromycin A N-oxide obtained above with a reducing agent in a high yield.
EP1683863A2 A method for enhancing neurone survival and agents useful for same Antisense oligonucleotides to nerve growth factor receptor, p75NOFR gene downregulate expression, thereby facilitating neurone survival.
US8552013 Heterocyclic compounds based on N6-substituted adenine, methods of their preparation, their use for preparation of drugs, cosmetic preparations and growth regulators, pharmaceutical preparations, cosmetic preparations and growth regulators containing these compounds Novel heterocyclic derivatives based on N6-substituted adenine, having anticancer, mitotic, immunosuppressive and antisenescent properties for plant, animal and human cells and methods of their preparation. Included are also pharmaceutical compositions, cosmetic preparations and growth regulators, which contain these derivatives as active compound and the use of these derivatives for the preparation of drugs, cosmetic preparations, in biotechnological processes, in cosmetics and in agriculture.
US7105573 Administering to the mammal an insulin sensitivity increasing substance (ISIS) in an amount effective to treat the disorder in the mammal, in a manner so as to reach an affected area of the pilosebaceous apparatus Insulin sensitivity increasing substances (ISIS), including but not limited to D-chiro-inositol, thiazolidinedione and derivatives, and biguanides, are useful in the treatment of hair loss and other disorders of the pilosebaceous apparatus (hirsutism, acne, etc.) associated with conditions of excess insulin and/or insulin resistance. The treatment comprises administering to a mammal, such as a human, at least one ISIS either alone or in combination with at least one agent, such as an androgen receptor blocker (ARB) and/or a steroid enzyme inhibitor or inducer (STI). Additionally, an activity enhancing agent may be included for topical administration.
EP1776119B9 Tetrahydro-naphthalene derivatives as glucocorticoid receptor modulators The present invention is directed to compounds of formula (I): wherein R represents a methyl or an ethyl group X represents N, C-H or C-CH3 when X represents C-H or C-CH3, Y represents N when X represents N, Y represents C-H and physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.
US7601748 Anti-androgenic pyrrolidines with tumor-inhibiting action This invention relates to anti-androgenic N-[ω-[3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituted pyrrolidines of general formula I, with a strongly pronounced antiproliferative profile of action; process for the production of the compounds of general formula I, pharmaceutical preparations and the use for the production of pharmaceutical agents.
CN101683344A Nutritious mixture of amino acid and vitamin for preventing hair losing and improving hair growing The invention provides a nutritious mixture of amino acid and vitamin for preventing hair losing and improving hair growing. The hair keratin of human body is composed of more than twenty amino acids,and sufficient supplement of these amino acid substances can synthesize and repair the hair keratin of human body effectively, and has special effect for preventing alopecia and promoting hair growing. Considering that most of the amino acid substances can be obtained in daily diet, so in the invention, kind and content of four main amino acid substances for composing hair keratin is provided, which are cystine, arginine, leucine, threonine in sequence of content. In view of some vitamin substances have very important effect to nutrition of human bari, for improving function effect of the invention, the invention also especially adding nicotinic acid, folic acid, pantothenic acid, inositol four vitamin substances and formulate the content.
CN103565778A Lutein microcapsule and preparation method thereof The invention relates to a lutein microcapsule and a preparation method thereof, wherein the lutein microcapsule consists of a core containing a lutein crystal and an oil soluble emulsifying agent, a shell covering the core, and starch grains stuck outside the shell; the shell includes a capsule material, a water soluble emulsifying agent and a stabilizing agent, wherein dosage ratio of the lutein crystal to the oil soluble emulsifying agent to the capsule material to the water soluble emulsifying agent to the stabilizing agent is (1-30): (0.5-5): (60-95): (1-8): (0.5-5) in parts by weight. The lutein microcapsule is regular in shape, relatively uniform in granularity, good in fluidity, and excellent in both stability and activity.
US20110034508 Treatment of BDNF-related disorders using laquinimod This application provides for a method of increasing brain-derived neurotrophic factor (BDNF) serum level in a human subject comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to increase BDNF serum level in the human subject. The method can further comprise periodically administering to the subject an amount of a second BDNF-increasing agent. This application also provides for a method for treating a human subject suffering from a BDNF-related disease comprising periodically administering laquinimod or a pharmaceutically acceptable salt thereof in an amount effective to treat the human subject. This application additionally provides for use of laquinimod in the manufacture of a medicament for increasing BDNF serum level in a human subject. This application further provides for a pharmaceutical composition comprising an amount of laquinimod effective for use in increasing BDNF serum level in a human subject. This application also provides for a pharmaceutical preparation comprising an amount of laquinimod and an amount of a second BDNF-increasing agent effective for use in increasing BDNF serum level in a human subject.
EP2358439A1 Methods for treating hepatitis c virus infection A method of treating a patient infected with HCV comprises administering to the patient VX-950 and interferon. In the method, an interferon trough level and/or a VX-950 trough level of the patient independently are monitored. The method further includes determining whether or not to adjust: subsequent administration of VX-950 to obtain a minimum target VX-950 trough level of about 1,500 ng/mL; subsequent administration of interferon to obtain a minimum target interferon trough level of about 5,000 pg/mL; or subsequent administration of VX-950 and interferon to obtain said minimum target trough levels.
US20110237667 Compositions Containing Diethanol Amine Esterquats The invention relates to compositions containing one or more compounds of the formula (1), wherein R1CO and R2CO are linear or branched saturated acyl groups independent of each other, having 18 to 24 C atoms, and A− is a counter-ion, and the total amount of C18-23-alkyl COO groups is 40.0 wt.-% or more, based on all groups R1COO— and R2COO—. The compositions are, for example, cosmetic, dermatological, or pharmaceutical compositions.
US7265106 Chromatography; separation of enantiomorphs (R)-tofisopam, substantially free of the (S)-enantiomer of tofisopam, is obtained by separating the enantiomers of tofisopam by chromatography employing a chiral separation medium comprising (i) (2S)-2-{(1S)[(3,5-dinitrophenyl)carbonylamino]phenylmethyl}-3,3-dimethylbutanoate, covalently bound to silica through an alkylene ester linkage or (ii) an amylose derivative of formula I: wherein each R1 and n are defined herein; the amylose derivative being coated on a porous inorganic carrier or a porous organic carrier.
WO2013133390A1 Anti-nephropathic drug A thiosugar sulfonium salt compound according to the present invention, which is represented by general formula [I], is effective against nephropathy, particularly diabetic nephropathy, and is therefore useful as an anti-nephropathic drug or an anti-nephropathic food for preventing or treating nephropathy. The thiosugar sulfonium salt compound according to the present invention, which is represented by general formula [I], also has an inhibitory activity on α-glucosidase, and is therefore useful as a medicine for preventing or treating diabetes-related diseases, such as a medicine for preventing or treating diabetes, diabetic complications, obesity, errors of lipid metabolism, hypertension or the like.
EP2625168A1 Phenyl diamides and a pharmaceutical preparation comprising phenyl diamides The present invention relates to phenyl diamides according to the general formula (1) and their use as a medicament and a pharmaceutical preparation comprising as an active ingredient a phenyl diamide according to the general formula (1). Further, the present invention relates to phenyl diamides according to the formulas (16), (17) and (18) for use in the treatment of gliomas.
US20120270943 D-aspartic Acid Pro-nutrients with Improved Solubility Characteristics D-aspartic acid is prepared as its hydrochloride salt or as the hydrochloride salt of its diethyl ester, thereby providing soluble forms of D-aspartic acid that are readily taken up by a human body via its digestive tract. The D-aspartic acid is administered as pills, capsules, powdered drink mixes, beverages, confectionaries, syrups, chewable tablets, nasal sprays, or injectable formulations.
CA2360676C A method for treating patients with acne by administering a cyclic gmp pde inhibitor Inhibitors of cGMP PDE are useful in the treatment of acne.
EP1511483A2 Methods of treatment with lxr modulators Disclosed are methods of using compounds that modulate LXR.
CN101991534A EPA (eicoeapentaenoieaeid) ester fat emulsion intravenous injection and preparation method thereof The invention provides an EPA (eicoeapentaenoieaeid) ester fat emulsion intravenous injection and a preparation method thereof. The EPA ester fat emulsion intravenous injection comprises the raw materials of EPA ester, lecithin, glycerol, aseptic pure water, antioxidant, stabilizer, pH regulator and the like, and the preparation method comprises the following steps: under the protection of nitrogen, mixing, violently stirring, shearing the stirred mixture at high speed into an initial emulsion, then emulsifying by a high-pressure homogenizer, filtering by a microporous membrane filter, filling, sealing and sterilizing to obtain the EPA ester fat emulsion intravenous injection. The used EPA ester is EPA methyl ester, EPA ethyl ester, EPA ehtylene, EPA propylene and EPA triglyceride, and the content of EPA is greater than 90%. The EPA ester fat emulsion intravenous injection is used in the fields of medical treatment and health, and can be applied to parenteral intravenous injection administration, or enteral tube feeding or oral administration as a trophic and therapeutic medicine.
CA2378503C Manufacture and use of an antibiotic/antibiotics(or: antibiotic(s)) preparation The present invention concerns the manufacture and use of an antibiotic/antibiotics preparation for human and veterinary medicine, for the treatment of local microbial infections in hard and soft tissue. The manufacture in accordance with the invention of an antibiotic/antibiotics preparation takes place according to the invention in that water, an amphiphilic component of a representative of the alkyl sulfates, aryl sulfates, alkylaryl sulfates, cycloalkyl sulfates, alkylcycloalkyl sulfates, alkyl sulfamates, cycloalkyl sulfamates, alkylcycloalkyl sulfamates, aryl sulfamates, alkylaryl sulfamates, alkyl sulfonates, fatty acid-2- sulfonates, aryl sulfonates, alkylaryl sulfonates, cycloalkyl sulfonates, alkylcycloalkyl sulfonates, alkyl disulfates, cycloalkyl disulfates, alkyl disulfonates, cycloalkyl disulfonates, aryl disulfonates, alkylaryl disulfonates, aryl trisulfonates and alkylaryl trisulfonates, one or more antibiotic components from the group of aminoglycoside antibiotics, lincosamide antibiotics and tetracycline antibiotics, an organic auxiliary component and/or an inorganic auxiliary component and if need be at least one biologically active component are mixed together and shaped into molded elements, granulates, powders, foils, shaped masses and threads.
US20080269209 P 38 map kinase inhibitor; autoimmune diseases; antiinflammatory agents; cardovascular disorders; bone disorders; neurodegenerative diseases; antiproliferative agents New compounds of formula I, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors. (I)
US7875342 Porous ceramic composite bone grafts The invention relates to porous ceramic composites incorporating biodegradable polymers for use as a bone substitute in the fields of orthopedics and dentistry or as a scaffold for tissue engineering applications. The porous ceramic composite implant for connective tissue replacement comprises a porous ceramic matrix having a biodegradable polymer provided on internal and external surfaces of the ceramic matrix. The biodegradable polymer allows for the passage and/or delivery of a variety of agents throughout the porous ceramic matrix and improves mechanical properties of the implant in vivo.
CN103272235A Pharmaceutical composition for preventing or treating cold injury and thrombus The invention belongs to the technical field of a medicine, relates to a pharmaceutical composition for preventing or treating cold injury and thrombus, and particularly relates to use of a pharmaceutical composition including an M cholinoceptor blocking drug and an alpha1 receptor antagonist drug, and use of the pharmaceutical composition for preparing a drug for preventing or treating the cold injury, chimatlon, thrombus or protecting vascular endothelial cells. The invention is confirmed that the cold injury can be effectively prevented or treated by combination of the M cholinoceptor blocking drug and the alpha1 receptor antagonist drug; the thrombus can be effectively reduced; the thrombus forming length is shortened; the pharmaceutical composition has the function of protecting the vascular endothelial cells; the effect is much superior to that of a single drug; and the two drugs have synergistic effects by combination.
US20120308563 Regulatory b cells (tbregs) and their use Regulatory B cells (tBreg) are disclosed herein. These regulatory B cells express CD25 (CD25+) a pan B cell marker such as B220 (B220+), and also express CD19 (CD19+). These regulatory B cells suppress resting and activated T cells in cell contact-dependent manner. Methods for generating these regulatory B cells are also disclosed herein, as are methods for using these regulatory B cells to produce regulatory T cells (Treg). In some embodiments, methods for treating an immune-mediated disorder, such as an autoimmune disease, transplant rejection, graft-versus-host disease or inflammation, are disclosed. These methods include increasing regulatory B cell number or activity and/or by administering autologous regulatory B cells. Methods for treating cancer are also disclosed herein. These methods include decreasing regulatory B cell activity and/or number.
US20080194630 LTA4H modulators and uses thereof Leukotriene A4 hydrolase (LTA4H) inhibitors, compositions containing them, and methods of use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and/or conditions associated with inflammation.
CN101940558A (-)-Epigallocatechin-3-gallate pill composition and application thereof The invention discloses a pill composition prepared by (-)-epigallocatechin-3-gallate as an active component and pharmaceutically acceptable adjuvant materials and application of the composition for preventing and curing senile dementia. The invention has an outstanding characteristic of providing a safe and effective controllable-quality convenient-use oral pill composition for senile dementia patients.
WO2010076564A3 Isochromenones useful in the treatment of inflammation This invention is directed to compounds of formula (I): wherein R1, R2, R3, Rx, Ry, m and n have meanings given in the description, or pharmaceutically acceptable salts, solvates or prodrugs thereof, which are useful as PDE4, PDE7 or PDE4 and PDE7 inhibitors, and therefore useful e.g. in the treatment and/or prevention of diseases and conditions associated with inflammation.
WO2011057580A1 Organic dicarboxylic acids, salts and preparation method thereof Organic dicarboxylic acid compounds, salts and preparation methods thereof. The said compounds have activity of resisting oxidation damage to crystalline lens of eyes. The structures of the above organic dicarboxylic acid compounds are shown as formula (1).
CN102247343A Preparation process of compound pioglitazone and metformin sustained-release tablets The invention discloses a preparation process of compound pioglitazone and metformin sustained-release tablets, belonging to the technical field of preparation of pharmaceutical sustained and controlled release formulations. The preparation process adopts metformin sustained-release matrix tablets with microporous film coatings, pioglitazone quick-release film coatings are externally coated, therefore, the quick-release film coatings quickly release the pioglitazone, and the sustained-release matrix tablets with microporous film coatings dually retard and control the metformin to slowly release for as long as 24 hours. The in vitro release characteristics of pioglitazone in the compound pioglitazone and metformin sustained-release tablets is: 50-70% in 5-10 minutes, 60-100% in 10-30 minutes, and 80-100% in 30-45 minutes; and the in vitro release characteristics of metformin is 0-30% in 1-3 hours, 30-60% in 2-8 hours, 60-80% in 8-12 hours and 80-100% in 12-20 hours. The process has a simple and safe procedure, controllable quality, low cost and short production cycle, and is suitable for large-scale industrial production.
CN101301291A Compound enrofloxacin injection for animals and preparation thereof The invention discloses a compound enrofloxacin injection for animals and a preparation method thereof, which aims to provide the enrofloxacin injection for the animals and the preparation method thereof, wherein, the enrofloxacin injection for the animals can treat swine enzootic pneumonia, is quick to take effect, decreases drug resistance, and can treat symptoms and root causes; and the preparation method has a simple process and is easy to realize. The injection comprises the following compositions by weight portion: 0.5 to 5kg of enrofloxacin, 1 to 10kg of lincomycin hydrochloride, 0.01 to 0.05kg of sodium hydroxide, 0.1 to 2kg of doxofylline, 0.2kg of sodium sulfite, 0.01kg of EDTA-2Na, 30kg of propanediol, and the balance being water for injection. The injection adopts a compound preparation of an antimicrobial drug and antibiotics; due to the combined use of the enrofloxacin and the lincomycin hydrochloride as well as the doxofylline, the injection is quick to take effect to the swine enzootic pneumonia, is effective and highly efficient, reduces the probability of the drug resistance, can apparently relieve clinical symptoms caused by the swine enzootic pneumonia, can treat symptoms and root causes, and increase the weight of pigs.
WO2006077856A1 Injection for mastitis An injection for mastitis which contains a main ingredient, a medium-chain fatty acid monoglyceride and an oily base, wherein the diffusion and dispersion of the main ingredient is accelerated by the medium-chain fatty acid monoglyceride so that the elution properties of the main ingredient are improved and the absorbability thereof is elevated. Thus, it is expected that the above-described injection exerts an immediate action and has a short retention time and, therefore, the main ingredient can be effectively utilized while reducing waste, compared with the existing injections for mastitis.
WO2008057252A3 Solid forms comprising 4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro-phenylamino)-9h-purin-2-ylamino]-cyclohexan-1-ol, compositions thereof, and use therewith Solid forms comprising 4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro- phenylamino)-9H-purin-2-ylamino]-cyclohexan-1-ol, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.
WO2007091644A1 Fungal growth inhibitor It is intended to provide a highly safe and useful fungal growth inhibitor and so on. More specifically, it is intended to provide: (1) a fungal growth inhibitor which comprises hyaluronic acid or its salt (excluding heavy metal salts) as the active ingredient, and a method of inhibiting the growth of a fungus which comprises at least the step of contacting the fungus with hyaluronic acid or its salt (excluding heavy metal salts); (2) an agent for potentiating the fungal growth inhibitory effect of a cell which comprises a DNA encoding hyaluronate synthase as the active ingredient; (3) a method of potentiating the fungal growth inhibitory effect of a cell which comprises at least the step of transferring a DNA encoding hyaluronate synthase into the cell; and (4) a method of inhibiting the growth of a fungus which comprises at least the step of contacting the fungus with a cell carrying a DNA encoding hyaluronate synthase that has been transferred thereinto.
US7722874 Methods for reducing T cell responsiveness to an autoantigen with anti-gp39 antibodies and antigen presenting cells Methods for inducing antigen-specific T cell tolerance are disclosed. The methods involve contacting a T cell with: 1) a cell which presents antigen to the T cell, wherein a ligand on the cell interacts with a receptor on the surface of the T cell which mediates contact-dependent helper effector function; and 2) an antagonist of the receptor on the surface of the T cell which inhibits interaction of the ligand on the antigen presenting cell with the receptor on the T cell. In a preferred embodiment, the cell which presents antigen to the T cell is a B cell and the receptor on the surface of the T cell which mediates contact-dependent helper effector function is gp39. Preferably, the antagonist is an anti-gp39 antibody or a soluble gp39 ligand (e.g., soluble CD40). The methods of the invention can be used to induce T cell tolerance to a soluble antigen or to an allogeneic cell. The methods of the invention can also be used to induce tolerance in cases of bone marrow transplantation and other organ transplants and to inhibit graft-versus-host disease.
WO2012070024A1 Carbonic anhydrase inhibitors with antimetastatic activity Compositions for the treatment of cancer comprising coumarin and thiocoumarin derivatives of Formulas I- XII are disclosed. Said derivatives preferentially inhibit carbonic anhydrase IX and XII (which are associated with hypoxic and metastatic tumours) over inhibiting carbonic anhydrase I and II activity. The compositions therefore are suited for treatment of hypoxic or metastatic cancers due to this selective mechanism of action.
CN102516244A Hexa-atomic aromatic heterocyclic imidazole mercapto-acetamide derivative, and preparation method and application thereof The invention belongs to the technical field of medicines and specifically discloses a hexa-atomic aromatic heterocyclic imidazole mercapto-acetamide derivative shown by the formula I, a pharmaceutically acceptable salt, ester or prodrug thereof, a preparation method thereof and an application of a compound containing one or more derivatives in the medicines for treating and preventing (Human Immunodeficiency Virus) HIV infection.
US20090215748 FXR agonists for treating vitamin D associated diseases Provided are certain methods of treating at least one condition that can be treated by elevating the vitamin D receptor (VDR) activity level in a patient with at least one farnesoid X receptor (FXR) agonist. Also provided are certain methods of modulating levels of Cytochrome P450, family 27, subfamily B, polypeptide 1 (CYP27B1) and 1α,25-dihydroxyvitamin D3 in cells, certain methods of modulating VDR activity levels, certain methods of modulating levels of an extracellular matrix protein, renin angiotensin system (RAS) pathway, parathyroid hormone, serum creatinine, serum albumin, proteinuria, lipid metabolism, renal lipid deposition, mesangial expansion, glomerulosclerosis, kidney inflammation, blood pressure, bone resorption, and bone formation, certain methods of identifying FXR modulators, certain methods of diagnosing the risk that a patient will develop at least one condition that can be treated by elevating the VDR activity level, and certain methods of characterizing the levels of FXR activity in mammals.
US20060178394 Inhalable dose of a powder comprising apomorphine or pharmaceutically acceptable salts thereof for therapy of for sexual dysfunction The present invention relates to inhalable formulations of apomorphine or its pharmaceutically acceptable salts or esters for use in treating sexual dysfunction. The present invention also relates to methods for preparing the apomorphine formulations as well as to methods for treatment of sexual dysfunction using said formulations and inhalers including said formulations. The present invention further relates to the use of apomorphine in the manufacture of a medicament for treating sexual dysfunction.
US7060705 2-(saturated N-heterocycylalkyl) quinazolinone compounds, e.g., 3-benzyl-2-[1-(4-methylpiperazin-1-yl)propyl]quinazolin-4(3H)-one, used to treat cancer, especially histiocytic lymphoma, lung adenocarcinoma, small cell lung cancer, pancreatic cancer, glioblastoma and breast carcinoma The present invention relates to quinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
CN102512655A L-carnitine composition, L-carnitine preparation and preparation method and application thereof The invention provides an L-carnitine composition, an L-carnitine preparation and a preparation method and application thereof. The composition can comprise L-carnitine or a salt thereof acceptable pharmaceutically, kreatine, branched-chain amino acid, glutamine and soybean peptide. The composition used for improving tolerance can increase the combustion of fat in a human body, effectively oxidize the fat in the human body and decompose the fat into energy, implements nutrition required by the human body, and improves the athletic ability.
CN101095943A Compound recipe human body bone component extender The invention relates to a new-type combined replenisher for human bone, which can adjust bone metabolism, replenishing calcium and peptide, promote bone growth and improve bone quality.
WO2008098196A1 Treprostinil treatment for interstitial lung disease and asthma The present invention describes methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and/or prevention of interstitial lung disease or asthma, or a condition, such as pulmonary fibrosis, associated with interstitial lung disease or a condition associated with asthma. The invention also relates to kits for treatment and/or prevention of such condition that include an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.
CN1748693A Albendazole jelly for treating chronic nasosinusitis The present invention relates to the preparation process of nasal albendazole jelly and the application of the nasal albendazole jelly in treating chronic nasosinusitis.
EP2711008A1 N6,N6-dimethyladenosine for use in treating or preventing primary and metastatic breast cancer The present invention relates to the field of biotechnology. The present invention relates to a compound of formula (I), namely N6,N6-dimethyladenosine, for use in the treatment or prevention of primary and metastatic breast cancer. The present invention also relates to a combination of a compound of formula (I) with at least one further compound for use in the treatment or prevention of primary and metastatic breast cancer. The present invention further relates to a pharmaceutical composition comprising the compound of formula (I) or the combination.
CA2228492C Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors Novel and known bicyclic 4-aralkylaminopyrimidine derivatives of formula (I) wherein A is a benzene or imidazole ring; B is a benzene, tetralin, indane or 2-oxindole ring R is (C1-C4)perfluoroalkyl, phenyl, phenyl-(C1-C4)alkyl, hydroxy-(C1-C4)alkyl, (C1-C4)alkoxy-(C1-C4)alkyl, (C2-C4)acyloxy-(C1-C4)alkyl, halobenzoyloxy-(C1-C4)alkyl, carboxy, carbamoyl, (C1-C4)alkoxycarbonyl, cyano, (C1-C4)alkylcarbonyl, carboxy-(C1-C4)alkyl, carbamoyl-(C1-C4)alkyl, (C1-C4)alkoxycarbonyl-(C1-C4)alkyl, halo-(C1-C4)alkyl, amino-(C1-C4)alkyl, mono- or di-(C1-C4)alkylamino-(C1-C4)alkyl, sulfo-(C1-C4)alkyl or sulfamido-(C1-C4)alkyl; each of R1 and R2, which may be the same or different, is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen or -NR5R6 in which each of R5 and R6, which may be the same or different, is H or C1-C4 alkyl; each of R3 and R4, which may the same or different, is hydrogen, C1-C4 alkyl, halogen, hydroxy, C1-C4 alkoxy, C1-C4 alkoxycarbonyl, nitro, cyano or CF3; and the pharmaceutically acceptable salts thereof, are tyrosine kinase inhibitors.
US8202860 Methods and compositions for treating primary and secondary tumors of the central nervous system (CNS) Methods and compositions for the treatment and/or prophylaxis and/or suppression of primary and/or secondary tumors of the central nervous system (brain and spinal cord, eyes) in mammalian subjects are disclosed, wherein an effective dose of a methylol transfer agent such as Taurolidine and/or Taurultam and/or a bioequivalent is administered to a mammalian subject suffering from, or at risk of growth of, tumors of the central nervous system. Furthermore, methods for local application of Taurolidine and/or Taurultam and/or a bioequivalent in solution are disclosed using microdialysis methods, irrigation methods, implantion methods and angiographic methods.
US20120095066 Composition Comprising An Epothilone And Methods For Producing A Composition Comprising An Epothilone The present invention concerns methods for the production of pharmaceutical formulations of Epothilones suitable for being administered parenterally, such as intravenously.
US8440682 4-benzylamino-1-carboxylacyl-piperidine derivatives as CETP inhibitors The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
CN103550188A Lansoprazole enteric-coated pellet capsule as well as preparation method thereof The invention relates to the field of preparations and specifically relates to a lansoprazole enteric-coated pellet capsule as well as a preparation method thereof. A technical problem to be solved in the invention is to provide a lansoprazole enteric-coated pellet capsule which is more stable and controllable in quality, and safer and more reliable for human body use. The lansoprazole enteric-coated pellet capsule comprises a pellet and a capsule shell, wherein the pellet is a pellet pill-containing core which is coated with an isolated coating layer and an enteric coating layer in sequence; the pellet pill-containing core comprises the following materials in parts by weight: 5-20 parts of lansoprazole, 30-80 parts of blank pill cores, 0.5-2 parts of a pH regulator, 1-3 parts of an adhesive and 25-45 parts of water, and a micronization particle size range of lansoprazole is preferably D95 equal to 5 mu m-8 mu m; the isolated coating layer is a mixture of a filling agent and an adhesive in a weight ratio of 1:2-1:6, or is gastric type Opadry; the enteric coating layer contains a film-forming agent and a pore-foaming agent in a weight ratio of 1:18-1:24, or is enteric type Opadry.
US8679736 Removal of adenine during a pathogen reduction process in whole blood or red blood cells by dilution The methods of this invention involve preventing the formation of a complex between adenine and riboflavin by reducing the amount of adenine in a solution containing blood or blood components to be pathogen reduced.
US20080207563 Synergistic sequential or simultaneous administration of erlotinib and a MEK inhibiting N-substituted-{2,5-dioxo-imidazolidin-1-yl}-3-phenyl-butyramide Disclosed are methods for synergistically inhibiting the proliferation of tumor cells by contacting the tumor cells with a MEK inhibitor compound and erlotinib, either sequentially or simultaneously. Also disclosed are methods for inhibiting the proliferation of tumor cells in a human, by administering to the human, sequentially or simultaneously, an amount of erlotinib and a MEK inhibitor compound, wherein the amounts are effective, in combination, to synergistically inhibit the proliferation of the tumor cells in the human.
US20080026087 Litchi Sinensis Extracts Containing Oligomeric Proanthocyanidins and Processes of Making Thereof A botanic extract of Litchi sinensis containing, based on active substance content, at least 15% by weight of an oligomeric proanthocyanidin of the OPC A2 type is disclosed. Processes of making such extracts containing at least 15% by weight of OPC A2 are also disclosed.
CN102846559A Pantoprazole sodium freeze-dry preparation and preparation method thereof The invention discloses a pantoprazole sodium freeze-dry preparation. The pantoprazole sodium freeze-dry preparation comprises, by weight, 1 part of pantoprazole sodium, 0.5-1.2 parts of mannitol, 0.02-0.1 part of edetate disodium, 0.03-0.06 part of sodium bisulfite, 0.01-0.02 part of sodium hydroxide and 50 parts of water for injection. The pantoprazole sodium freeze-dry preparation has the advantages that the stability of the pantoprazole sodium is increased, degradation of the pantoprazole sodium is suppressed, and accordingly bioavailability and safety are improved.
EP1637135A1 Compositions comprising dimethylsulfoxide and tretinoin for treating skin disorders Compositions and methods for treatment of skin conditions, such as age spots, liver spots, photodamaged skin, skin folds, diminished hair growth, non-infectious cellulite and "orange skin", or for repairing damaged DNA in a skin cell, utilize a formulation including about 0.01-1 part by weight tretinoin, and about 1-45 parts by weight dimethylfsulfoxide. Compositions may include about 5-40 parts by weight urea, and about 45-90 parts by weight carrier.
WO2008066102A1 Sustained release preparation Disclosed is a sustained release preparation which is prepared by shaping a granule comprising a blood coagulation factor Xa inhibitor and a mixture of at least two hydrophilic polymers. Also disclosed is a pharmaceutical composition comprising a combination of the sustained release preparation and an immediate release preparation comprising a blood coagulation factor Xa inhibitor. It becomes possible to provide a controlled release preparation comprising a blood coagulation factor Xa inhibitor for the prevention or treatment of thrombosis, which can control the activity of blood coagulation factor Xa for a long term and is excellent in convenience and compliance. It is also becomes possible to provide a method for producing the controlled release preparation.
US20140072607 Polycarbonates bearing pendant primary amines for medical applications An antimicrobial composition comprises an anionic drug and an amine polymer comprising a first repeat unit of formula (2): wherein a′ is an integer equal to 1 or 2, b′ is an integer equal to 1 or 2, and each R′ is an independent monovalent radical selected from the group consisting of hydrogen, methyl, ethyl, and combinations thereof. G′ is a divalent linking group selected from the group consisting of a single bond and groups comprising at least one carbon. X− is a negatively charged counterion. The drug and the amine polymer are bound by noncovalent interactions.
US7141542 Biologically active protein useful for aerosol delivery to the respiratory tract The invention is directed to a stable formulation of a biologically active protein useful for aerosol delivery to the respiratory tract of a patient in need of treatment comprising: (a) a carrier liquid comprising from about 10% to from about 100% V/V water and from about 0% to from about 90% V/V of an organic liquid; (b) a biologically effective amount of a protein suspended or dissolved in a carrier liquid; and (c) a stabilizing effective amount of a derivatized carbohydrate stabilizing agent suspended or dissolved in said carrier liquid. The stable formulations of the invention may optionally contain about 0.1% to about 5.0% W/V of a pharmaceutically acceptable excipient.
EP1732545A1 Tetrahydro-beta-carboline compounds and use thereof Tetrahydro-ß -carboline compounds represented by the following formulae: Wherein x, y and z are each independently an integer of 0 to 4 and R is selected from the group consisting of H, alkyl, aryl and heterocyclic moiety wherein the alkyl, aryl and heterocyclic moiety are optionally substituted with a member selected from the group consisting of halogen, alkoxy and trifluoromethyl; pharmaceutically acceptable salts thereof and prodrugs thereof are provided. The compounds are useful for treating neurological diseases.
WO2008144665A1 Use of pimavanserin in the treatment of parkinson and symptoms thereof It is shown that pimavanserin can be administered with or without food without significant effect on absorption or pharmacokinetics. It is also shown that pimavanserin can be used to treat Parkinson's disease psychosis without significantly worsening motor symptoms.
US20070060544 4-Nitro-2-[(4'-methoxy)-phenoxy]-methanesulfonanilide derivatives and their pharmaceutical use 4-nitro-2-[4′-methoxy)-phenoxy]-methane-sulfonanilide or the pharmaceutical acceptable salts or solvates or hydrates thereof are provided. Also provided is their mixture with povidone, phospholipids or cyclodextrin, as well as their pharmaceutical uses, particularly the use as a non-steroidal anti-inflammatory, analgetic agent.
WO2010058824A1 Substance for regulating differentiation into mesenchymal cell, and use thereof Disclosed is a regulator which can act on the process of the differentiation of an osteoblast or the like specifically to regulate the differentiation of the osteoblast or the like. Also disclosed is use of the regulator. Specifically disclosed is a regulator for the differentiation into a mesenchymal cell, which comprises an active ingredient selected from miRNA that can bind to a 3'-untranslated region in Dlx5 gene, a precursor of the miRNA, a DNA construct that encodes the miRNA or the precursor of the miRNA, and an inhibitor of the miRNA.
WO2014018919A1 Seriniquinones, melanoma-specific anticancer agents Accordingly, there are provided, inter alia, derivatives of seriniquinone and methods useful for the treatment of cancer, and in particular treatment of melanoma and prostate cancer.
CN1754534A Lysine hydrochlorate for injection and its preparation method The invention relates to a lysine hydrochloride for injection and its preparing process, which is a solution of certain concentration prepared from lysine hydrochloride as raw material or right amount of assisting solvent. The preparing process consists of degerming through film filtration method, computing the amount and freeze drying repeatedly. The obtained injection has good stability.
WO2009134723A9 Progesterone antagonists such as cdb-4124 in the treatment of breast cancer The subject matter of the instant invention is pertinent to the field of cancer treatment. In particular, the instant invention is relevant to the treatment and/or prevention of breast cancer in a patient. Compositions for practicing the methods, comprising selective progesterone receptor modulators, which function as progesterone agonists in the uterus and as progesterone antagonists in the breast tissue and exhibit only low affinity for glucocorticoid and estrogen receptors, are also disclosed. Embodiments of the instant invention also disclose methods for preventing the development of breast cancer in patients undergoing hormone replacement therapy or estrogen therapy.
WO2010114896A1 Substituted indolo-pyridinone compounds The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
US20090105212 Immunomoderators; antiallergens; viricides; bactericides; anticancer agents; rhinitis; hepatitis; skin disorders A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1, L2, and L3 each independently represents linear or branched alkylene, etc.; R1 represents (un)substituted alkyl, (un)substituted aryl, etc.; R2 represents hydrogen or (un) substituted alkyl; R3 represents (un)substituted alkyl, etc., provided that R3 may be bonded to L2 or L3 to form a nitrogenous saturated heterocycle; and X represents oxygen, etc.; or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.
CN103751184A Application of pregnane X receptor antagonist in preparation of lipid regulation and liver protection product The invention discloses application of a pregnane X receptor antagonist in preparation of a lipid regulation and liver protection product. The experiment results show that gomisin E has the effect of counteracting pregnane X receptors of human and rodent; as the suppression on growth of new lipid, reduction of ingestion of liver cell to free fatty acid, and up-regulation of gene related to fatty acid beta-oxidation, the content of triglyceride in liver of a high-fat diet induced fatty liver animal model is obviously lowered down, and the pathological change of the tissue of the fatty liver animal model is greatly improved; and gomisin E can also be used for preventing liver damage caused by chemical medicines (acetaminophen, rifampicin and isoniazide). According to the application, a chemical entity is provided, which is clear in target point, has no cellular poison, and can prevent fatty liver, hypercholesteremia and chemical liver injury; and the chemical entity can be individually used for preparing lipid regulation and liver protection product medicines, and also can be mixed with other components to prepare health foods.
CN103724313A Antineoplastic compound extracted from cambogia and preparation method and application of antineoplastic compound The invention relates to an antineoplastic compound extracted from cambogia and a preparation method and application of the antineoplastic compound. The preparation method comprises the following steps: (1) taking a medicinal material of the cambogia and extracting by using ethyl acetate, and conducting silica gel column chromatography separation and petroleum ether-ethyl acetate gradient elution on an extractive to obtain eleven constituents from A to K; (2) removing a grease constituent and a gambogic acid constituent, and conducting HPLC-PDA-MS repeat removing analysis to obtain a key constituent I; (3) conducting silica gel column chromatography separation and chloroform-methyl alcohol gradient elution on the constituent I to obtain a fraction I-3; (4) conducting inverse gas RP-18 chromatography separation and acetonitrile-water gradient elution on the I-3 to obtain a sub fraction I-3E; (5) conducting purification and acetonitrile elution on the I-3E to obtain the antineoplastic compound. The antineoplastic compound provided by the invention can be used for treating tumour.
US8772469 Synthetic double-stranded oligonucleotides for specific inhibition of gene expression The present invention relates to oligonucleotide derivatives which are at least partly double-stranded and which have a 2′5′-linked oligonucleotide residue on at least one 3′ end and to the use thereof for specific inhibition of gene expression.
CN101367812A Sulfhydryl pyrrolidine formamido cyclopentene acid substituted penem derivant The present invention belongs to the technical field of medicine, in particular to a penem derivative substituted by mercaptopyrrolidine formamidocyclopentene acid shown in the formula (I) and a pharmaceutically acceptable salt, an easily hydrolyzed ester, an isomer, a hydrate and a hydrate of the ester or the salt thereof: wherein, R<1>, R<2>, R<3>, R<4> and R<5> are defined in the description. The present invention also relates to preparation methods of the compounds, drug combinations and applications of the compounds in the preparation of drugs for treating and/or preventing infective diseases.
WO2006059897A1 Sphingolipids in treatment and prevention of steatosis and of steatosis or of hepatotoxicity and its sequelae The present invention relates to the use of sphingolipids for the preparation of a food item, a food supplement and/or a medicament for the prevention and/or treatment of hepatotoxic effects such as hepatic steatosis, fibrosis and/or cirrhosis. In particular, the invention relates to the use of a sphingolipid with the general formula (I): wherein Z is R3 or -CH (OH) -R3; A is sulphate, isulphonate, phosphate, phosphonate or -C (O) O-; Rl is H, hydroxyl, alditol, glycosyl, an alcohol, C1-C6 alkyl or amino acid; R2 is H or unsaturated or saturated (C1-C30) alkyl chain; R3 is unsaturated or saturated (C1-C30) alkyl chain; Ql is a primary amine group (-NH2), secondary amine group (-NH-) or an amide group ( -NH-CO-); and t is 0 or 1, or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the prevention and/or treatment of hepatotoxic effects such as hepatic steatosis, fibrosis and/or cirrhosis.
US20100137442 Sustained Release Particulate Oral Dosage Forms of (R)-Baclofen and Methods of Treatment Sustained release particulate oral dosage forms of (R)-baclofen prodrugs and methods of treating a disease comprising orally administering such dosage forms are disclosed.
WO2008081477A1 3-aryloxy 3-substituted propanamines Present invention relates to novel 3-aryloxy 3-substituted propanamines of formula (I), method of preparing the same and to their use in inhibiting serotonin and norepinephrine reuptake wherein A is a phenyl which is optionally substituted with up to five substituents; a 1- or 2-naphthyl which is unsubstituted or substituted; a 5-membered heteroaryl radical which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl, or substituted phenyl and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen; a 2-benzimidazolyl optionally unsubstituted or substituted; and R1 and R2 are each independently hydrogen, C1-6-alkyl, C3-7-cycloalkyl, C3-6-cycloalkyl C1-3-alkyl; or R1 and R2 may together form a C5-7-carbocyclic ring containing 0-2 hetero atoms such as N, O, or S and a salt thereof with a pharmaceutically acceptable acid. Compounds of formula (I) (I-A: R=4-CF3, R1=H, R2=CH3, A=4-fluorophenyl), I-B: R=4-CF3, R1=H, R2=CH3, A=4-methylphenyl, I-C: R=4-CF3, R1=H, R2=CH3, A=4-methoxyphenyl) are found to be better than the antidepressant drug fluoxetine.
EP1606244A2 Cycloalkylamides and their therapeutic use as antiepileptic and anticonvulsant The present invention relates to the use of compounds of formula (I)for the treatment of a variety of disorders including, bu t not limited to, epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, neuroprotection, and movement disorders.
US20080107755 Administer sodium selenite with an antioxidant to subject with reduced expression of Gadd45b in cerebral cortex, liver, intestinal, skeletal muscle tissue; antioxidant is alkylated diphenylamines, N-alkylated phenylenediamines, phenyl- alpha -naphthylamine; Alzheimer's, Pick's disease, supranuclear palsy The present invention relates to compositions and methods for altering cell function. In particular, the present invention provides compositions comprising selenium (e.g., SEL-PLEX) and methods of using the same (e.g., as a therapeutic and/or prophylactic treatment). Additionally, the present invention demonstrates that specific forms of selenium (e.g., SEL-PLEX), when administered to a subject, possess the ability to alter (e.g., reduce) gene expression in various tissues (e.g., compared to expression in subjects not administered selenium).
WO2014038623A1 3-(4-piperidyl)-indazole derivative Provided is a therapeutic agent for diseases associated with central nervous system (CNS) and/or peripheral nervous system (PNS) cholinergicity, diseases associated with smooth muscle contraction, endocrine diseases, diseases associated with neurodegeneration, and the like, said therapeutic agent comprising a compound represented by formula (I) [wherein R1A to R1D are the same as or different from one another and independently represent an optionally substituted C1-6 alkyl group or the like; R2 represents a hydrogen atom or the like; R3A to R3E are the same as or different from one another and independently represent a hydrogen atom or the like; R4 represents an optionally substituted C1-10 alkyl group or the like; and n represents 1 or 2] or a pharmaceutically acceptable salt thereof and having a potent action of regulating an α7 nicotinic acetylcholine receptor (α7 nAChR).
WO2007096151A3 Inhibitors of p38-kinase for treatment of pulmonary hypertension The use of a compound of formula A or a pharmaceutically acceptable derivative thereof for the manufacture of a medicament for the treatment of pulmonary hypertension, where R1, R2, R5, R6, B, C, D and G have the meanings described herein. Pharmaceutical compositions that contain the compounds are also described.
WO2013008909A1 Loxoprofen sodium-containing adhesive patch for external applications Provided is a loxoprofen sodium-containing adhesive patch for external applications, which has high transdermal absorbability of the main ingredient contained therein and has high stability so that the production of any decomposition product can be prevented during storage. An adhesive patch for external applications, comprising a support and an adhesive agent layer arranged on the support and containing 0.1 to 10 wt% of loxoprofen sodium, wherein the adhesive agent layer comprises 5 to 30 wt% of a styrene-isoprene-styrene block copolymer, 10 to 50 wt% of an alicyclic saturated hydrocarbon resin, 0.1 to 1 wt% of lactic acid and 5 to 15 wt% of a higher fatty acid and the ratio of the content of lactic acid to the content of the higher fatty acid (i.e., (lactic acid)/(higher fatty acid)) is 1/50 to 1/5.
CN101978981A Medicinal composition for treating oral ulcer and preparation method thereof The invention relates to a medicinal composition for treating oral ulcer and a preparation method thereof. The medicinal composition consists of raw medicaments such as root of pseudo-ginseng, hemsleyadin, borneol, dried alum, chlorhexidine and the like. The medicinal composition has broad-spectrum sterilization and bacteriostatic effects, is mainly used for disinfecting the oral ulcer, relieving pain and promoting healing, and has remarkable effect in many years of clinical application.
CN102885819A Application of evodiamine to preparation of anti-ultraviolet composition The invention provides application of evodiamine 57 to the preparation of an anti-ultraviolet composition, and also provides an anti-ultraviolet composition. The composition contains evodiamine 57 taken as an active ingredient, and one or more auxiliary materials externally applied to skin.
CN1579416A Medicinal composition for treating liver disease, its prepration method and use The invention discloses a medicine compound for curing hepatitis, which includes following ingredients and proportion: glycyrrhetic acid monoamine 1-200 shares, L-hydrochloric acid cysteine 1-200 shares, and one of sodium chloride, anhydrous sodium sulfite and ethylenediamine sodium acetic acid or the compound of then, the sodium chloride is 1-1000 shares, the anhydrous sodium sulfite is 1-200 shares, the ethylenediamine sodium acetic acid is 1-100 shares; it also discloses the medicine compound and the manufacturing method and the use, the medicine is compound solution, it can be applied to liver poisoning resisting, reduces the transaminase, recovers the functions of cell; it is mainly applied to cure the chronic hepatitis.
CN101602753B Ester compound in Neem oil as well as preparation method and application thereof The invention relates to an ester compound in Neem oil as well as a preparation method and an application thereof. Three saturated and/or unsaturated monoester or diester novel compounds are obtained by extracting a chloroform extract of the seed extract Neem oil of Azadirachtaindica A.Juss). Tests prove that a monomer or a mixture of the three compounds can be used as an antimicrobial medicine, an antiparasitic medicine and an antifertility medicine.
US20110045069 Precursor compounds of sweet taste receptor antagonists for the prevention or treatment of disease A description is given of precursor compounds of sweet taste receptor antagonists for the prevention or treatment of disease, in particular for the prevention or treatment of Type 2 diabetes. A description is also given of uses of these precursor compounds and edible compositions, preparations for nutrition or pleasure or semi-finished products and pharmaceutical preparations, containing such precursor compounds.
WO2008033431A1 Spirocyclic azetidinone derivatives for the treatment of disorders of lipid metabolism, pain, diabetes and other disorders The present invention relates to Spirocyclic Azetidinone Compounds, compositions comprising a Spirocyclic Azetidinone Compound and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of a Spirocyclic Azetidinone Compound.
US20100016393 Novel hydrogen sulfate salt The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation. Compound I
US20120029029 Substituted thiazol-2-ylamine derivatives, pharmaceutical compositions, and methods of use as 11-beta hsd1 modulators The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11βHSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable.
WO2013017619A1 Diphenyl substituted cyclohexane derivatives, useful as modulators of the estrogen receptors beta Disclosed herein are novel di-aromatic compounds of the general formula (I). Also pharmaceutical compositions comprising the novel compounds and the use of the novel compounds in treatment and prevention of diseases and disorders related to estrogen receptors are disclosed. Furthermore, methods for treating and preventing diseases and disorders related to estrogen receptors by administration of the novel compounds are disclosed.
US7285535 Administering TIRAP to block Toll/Interleukin-1 Receptor Adaptor Protein signaling in a cell; for treatment of inflammation and inducing or affecting immune response. TIRAP polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing TIRAP polypeptides and polynucleotides in therapy, and diagnostic assays for such.
CN101181575B Motherwort strip containing natural aromatic plant The invention relates to a motherwort strip which contains natural fragrant plant, comprising 85 to 95 parts of motherwort, 5 to 10 parts of menstruation regulating grass, 3 to 5 parts of peach blossoms, 2 parts of fructus amomis, 2 parts of banksian roses and 2 parts of sodium carboxymethyl celluloses. The invention is a composite, wherein, the motherwort has the effects of promoting blood circulation, regulating menstruation, inducing diuresis for removing edema and having direct effects on irregular menstruation, menoschesis, postpartum bruising pain, never-failing lochia, injuries from falls, pain skin ulcer and pyogenic infections, cutis pruriginosa, edema and difficult urination; the fructus amomi has the effects of eliminating dampness, dispelling cold, expelling phlegm and preventing recurrence of malaria; the menstruation regulating grass has the effects of regulating menstruation and removing blood stasis; the peach blossom has the effects of inducing diuresis, promoting blood circulation and relaxing bowels, etc; and the banksian rose has the effects of promoting circulation of qi and relieving pain. In addition, the invention can be matched with the well-known activating collaterals and warming moxibustion apparatus for using so as to carry out safe and healthy adjustment, physical therapy, health care and skin beautifying and maintenance on the human body. The invention has remarkable physical therapy effect, pleasant fragrance and low cost.
WO2011095095A1 Medicinal composition comprising alcohol-soluble and water-insoluble licorice extract, pharmaceutical preparation, pharmaceutical application, therapeutic method, and preparative method thereof A medicinal composition comprises the alcohol-soluble and water-insoluble licorice extract and at least one of antineoplastic agents or one of glucose-lowering and lipid-lowering medicines. The composition has synergistic effect in resisting tumor or reducing blood sugar and blood lipid. Moreover, the present invention provides the pharmaceutical preparation, pharmaceutical application, therapeutic method, and preparative method related to the medicinal composition.
CN101028280A Lavage liquor preparation for operation and its production A lavation liquid for ophthalmic operation, surgical operation, or abdominal chemicotherapy is proportionally prepared from sodium hyaluronate, water-soluble chitose and buffering phosphate solution. Its preparing process is also disclosed.
US7625943 5-alkyl-7-alkylcarbonate-isoflavone ester and related method A compound is provided for increasing the concentration of a parent isoflavone in a subject in vivo. The parent isoflavone has a skeletal structure including a 5 position and a 7 position, a 5 alkyl group, and a 7-hydroxy group with a 7-hydroxy oxygen appended to the 7 position and a 7-hydroxy hydrogen appended to the 7-hydroxy oxygen. The compound includes a substrate having the skeletal structure of the parent isoflavone, with a 5 position and a 7 position corresponding to the 5 and 7 positions respectively of the parent isoflavone. An alkyl group is appended to the 5 position. A promoiety is appended to the 7-hydroxy oxygen of the substrate as a substitute for the 7-hydroxy hydrogen of the parent isoflavone the promoiety and the 7-hydroxy oxygen establishing an alkylcarbonate ester. A related method also is provided.
EP1373241B1 Method for producing optically active dihydropyrones The invention relates to a novel method for producing optically active dihydropyrones, novel intermediate products obtained by said synthesis, and the use of the same as parent compounds in the production of pharmaceutically active compounds of formula 1-salt wherein R?1 and R2¿ independently represent hydrogen or a radical selected from the group consisting of C¿1?-C4-alkyl, C3-C8-cycloalkyl, C6-C10-aryl and C1-C4-alkylene-C6-C10-aryl, which can optionally be substituted once, twice or three times by means of at least one radical selected from the group consisting of hydroxy, halogen, C1-C4-alkoxy and CF3; R?3, R3', R4 and R4'¿ are the same or different and represent hydrogen or a radical selected from the group consisting of C¿1?-C4-alkyl, C3-C8-cycloalkyl, C6-C10-aryl and C1-C4-alkylene-C6-C10-aryl, which can optionally be substituted once, twice or three times by means of at least one radical selected from the group consisting of hydroxy, halogen, C1-C4-alkoxy, S-C1-C4-alkyl, SO2-C1-C4-alkyl, NO2 and CF3, optionally in the form of the tautomers thereof, provided that R?1 and R2¿ cannot simultaneously have the same designation, that when R?3 and R3'¿ have the same designation, the radicals R?4 and R4'¿ cannot have the same designation, and that when R?4 and R4'¿ have the same designation, the radicals R?3 and R3'¿ cannot have the same designation.
WO2006062110A1 Piperazine derivative A compound represented by the formula (I): [wherein R1 represents C3-9 branched alkyl; R2 represents, e.g., linear or branched, C2-9 alkyl optionally substituted by halogen, etc.; and X represents oxygen, etc.] (provided that the following cases are excluded: the case where R1 is tert-butyl, R2 is 2-methylpropyl, phenyl, tert-butyl, benzyl, or cyclohexyl, and X is oxygen and the case where R1 is tert-butyl, R2 is adamantly, neopentyl, or cyclohexylethenyl, and R3 is a single bond); or a pharmaceutically acceptable salt of the compound. The compound and salt have inhibitory activity against metabotropic glutamate receptor 1. They are hence useful for the treatment of diseases such as convulsion, acute pain, inflammatory pain, chronic pain, psychofunctional disorders including schizophrenia, and anxiety.
CN102805748A Pazufloxacin mesilate medicinal preparation and preparation method thereof The invention provides a pazufloxacin mesilate oral medicinal preparation which comprises the components by weight as follows: 8-15 parts of pazufloxacin mesilate, 0.7-2.0 parts of diluent 0-2.0 parts of a disintegrating agent, 0.03-0.1 parts of lubricant, 0.06-0.2 parts of glidant, 0-0.2 parts of an antisticking agent and 0.18-0.6 parts of adhesive. The preparation is simple in prescription and process, low in production cost, and high in stability and bio-availability, and completely meets the requirements of pharmacopeia. The invention provides a novel pazufloxacin oral medicinal preparation which is more safe and stable and more convenient for being taken.
WO2013053273A1 Imidazo quinoline derivative and medicinal salt thereof, preparation method thereof and use in medicine thereof The present invention relates to an imidazo quinoline derivative and a medicinal salt, a preparation method and the use in medicine thereof. In particular, the present invention relates to an imidazo quinoline derivative as shown in general formula (I) and a medicinal salt thereof, a preparation method thereof, and the use of both as a cancer therapeutic agent, especially the use as an inhibitor of mTOR and/or PI3K-kinase, wherein the definition of each substituent group in general formula (I) is the same as that in the description.
US20060057076 Oral humectants The invention provides a mouth wetting agent and a mouth wetting agent for false teeth including a safe and easily usable polymer composition and capable of relieving symptoms of dry mouth by maintaining the wetting properties of an oral cavity and the stability of false teeth. The mouth wetting agent of the invention includes a polymer composition containing a pharmaceutically acceptable water-soluble polymer, a pharmaceutically acceptable polyvalent alcohol and water and/or artificial saliva.
US20050143470 therapeutic treatment of Porcine Respiratory Disease Complex (PRDC) in pigs and Bovine Respiratory Syndrome (BRS) in calves; oral treatment; veterinary medicine The supplemented feed comprises a feed for animals supplemented with ketoprofen, and is useful for the oral treatment of conditions causing fever, inflammation and/or pain, simultaneously in a herd of animals.
CN1911922A Compound separated from petroleum ether extract of glycyrrhiza legume bacteria strain CCNWGX022 fermentation liquid The present invention discloses compound separated from licorice rhizobium strain CCNWGX022 fermenting liquid with petroleum ether extractant. The compound is named as 12-carbonyl-stearic acid-gamma-lactone, and has the structural expression as shown, molecular formula of C18H32O3, and molecular weight of 296. The compound has strong bacteria inhibiting effect, and minimum inhibiting concentration on both Staphylococcus aureus CMCCB26001 and Esaherichia coli CMCCB44102 of 100 mcg/ml.
CN101973925B 2-indolone compound with anti-inflammatory activity, preparation method and medicinal application thereof The invention relates to the medicament field, in particular to a new 2-indolone compound and a preparation method thereof. The invention also discloses a medicinal composition containing the compound and application thereof in treating inflammatory diseases such as rheumatic arthritis, rheumatoid arthritis, osteoarthritis and the like and treating other diseases or symptoms by inhibiting activities of cyclooxygenase (COX) and 5-lipoxygenase (5-LOX).
WO2007071850A3 Inhibition of the anti-fviii immune response The invention relates to a compound capable of inhibiting the endocytosis of FVIII (factor VIII) by immune system cells capable of endocytosing the antigen and to the therapeutic use of such a compound for the manufacture of a medicament for use in the treatment of haemophiliacs in order to reduce the immunogenicity of FVIII and/or increase the half-life of FVIII.
WO2006092209A1 Novel targets and compounds useful in the treatment of a cardiovascular disorder, dyslipidemia and atherosclerosis, and methods to identify such compounds The present invention provides targets and methods for the screening for compounds useful in the prevention, amelioration or treatment of a cardiovascular disorder, dyslipidemia, and/or Atherosclerosis. The invention also relates to the targets that were identified. Inhibiting target genes of the invention, or their expression products, by using compounds identifiable by methods of the invention, is beneficial in the treatment of diseases involving a cardiovascular disorder, dyslipidemia, and/or Atherosclerosis.
US20100247548 Antagonists of ci-m6p/igf2r for prevention and treatment of ctgf-mediated ocular disorders Antagonists of cation-independent mannose 6-phosphate/insulin-like growth factor-II receptor are provided for attenuation of CTGF signaling in a method of down-regulation of receptor signaling and downstream decreased signaling of connective tissue growth factor in ocular disorders involving inappropriate CTGF signaling. Ocular disorders involving inappropriate CTGF signaling include ocular hypertension, glaucoma, glaucomatous retinopathy, optic neuropathy, macular degeneration, diabetic retinopathy, choroidal neovascularization, and proliferative vitreoretinopathy, for example. Such disorders are treated by administering antagonists of the present invention.
EP2322173A1 Cationic bacteriochlorophyll derivatives and uses thereof The invention provides cationic tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one positively charged group and/or at least one basic group that is converted to a positively charged group under physiological conditions, preferably Bchls having an onium group derived from a N-containing aliphatic or heterocyclic radical such as ammonium, guanidinium, imidazolium, pyridinium, and the like or a phosphonium, arsonium, oxonium, sulfonium, selenonium, telluronium, stibonium, or bismuthonium group, or a basic group that is converted to such onium groups under physiological conditions, said groups being bound to one or more of the positions 173, 133 and 32 of the Bchl molecule by ester or amide bond. The Bchls are useful for photodynamic therapy and diagnosis.
US20060058379 Connexin 26 inhibitor and cancer metastasis inhibitors A connexin 26 inhibitor and a cancer metastasis inhibitor have a cis-oxirane structure and a terminal amide structure as represented by the following general formula (1): where R is a hydrogen atom or a hydrocarbon group, X is one of a hydrogen atom, a methansulfonyl group, an ethansulfonyl group, an acetyl group, a trifluoroacetyl group, a hydroxyl group, an alkoxy group and an amino group; m is an integer of from 4 to 10; and n is an integer of from 4 to 7. This compound is a novel cancer metastasis inhibitor which specifically inhibits the function of connexin 26.
US20110257207 Raf inhibitors The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are inhibitors or kinases such as Raf, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
US20060089355 Methods of treating alzheimer's disease using aromatically substituted w-amino-alkanoic acid amides and alkanoic acid diamides Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting de-position of A beta peptide in a mammal, by use of compounds of formula (I) wherein the variables R1, R2, R3, R4, R5, X1, and X2 are defined herein.
EP2768799A1 Substituted biaryl alkyl amides Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds.
WO2006070001A1 Substituted indole ligands for the orl-1 receptor New ligands for the ORL-1 receptor are described, useful for antagonising the activity of said receptors in a patient in need thereof, and for preventing and treating illnesses dependent on the activation of this receptor. The new compounds conform to structural formula (I) wherein R1 , R2, R3, R4 are further defined in the description.
US20050119162 Anxiolytic agents; using transferrins; quality of life for cancer patients; antiarthritic agents; antiinflammatory agents; compaction; uniform particle size The object of this invention is to provide a novel pharmaceutical composition for getting rid of pains and anxiety in patients. This invention relates to a pharmaceutical composition containing lactoferrin as an active ingredient. The composition of this invention is useful for treatment of at least one disease or condition selected from the group consisting of pains, including the phase 1 pain and the phase 2 pain, anxiety and stress. The composition is particularly beneficial to alleviating or getting rid of the pain and anxiety which significantly lower quality of life of patients with end-stage cancer. The composition of this invention is also useful for treatment of pains, including the phase 1 pain and the phase 2 pain, and inflammation which accompany arthritis or diseases in the junctions of bones (e.g. rheumatoid arthritis, osteoarthritis, frozen shoulder, sports injuries such as tennis elbow and baseball shoulder, and low back pain).
CN101190205A Ribavirin dissolvable tablet for infant The invention relates to a ribavirin soluble tablet which is a specification special for children, the components of which include effective dosage of ribavirin and the water-soluble medicinal excipient which can rapidly disintegrate in water and release medicine. When the tablet is taken by patients, the dosage of administration can be determined according to the weights of patients, therefore, the intake dosage of medicine can be more accurate and the safety can be improved. The invention is a beverage with sweet and sour taste when being dissolved, so the invention is easy to be accepted by children in term of the way of administration. Meanwhile, the solution of the medicine is beneficial for full absorption and is high in bioavailability.
WO2010045306A2 Azine derivatives and methods of use thereof The present invention relates to Azine Derivatives, pharmaceutical compositions comprising the Azine Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
US20110274644 Lens care compositions The present invention provides a lens care composition having a persistent lipid removal efficacy characterized by that the amount of lipids adsorbed by a silicone hydrogel lens after about 10 cycles of soiling with a lipid soiling solution and subsequent cleaning with a lens care solution of the invention under no-rubbing conditions is about 70% or less of that after about 10 cycles of soiling with the lipid soiling solution and subsequent cleaning with an aqueous phosphate buffer under no-rubbing conditions. The lens care composition comprises at least one surfactant, a polyvinylpyrrolidone (PVP), xylitol, a buffering agent, wherein in combination with polyvinylpyrrolidone (PVP) and xylitol, the surfactant provides the persistent lipid removal efficacy.
US20110034486 Use of pterocarpans as active anti-cellulite ingredients The invention relates to a cosmetic, dermatological or pharmaceutical preparation, containing one, two or more compounds of formula (I) and/or a pharmaceutically acceptable salt of a compound of this type, (i) for use in a method for preventing, treating or reducing cellulite, and/or (ii) in an adequate quantity to reduce the lipid quantity contained in subcutaneous fat tissue, and/or to inhibit the differentiation of preadipocytes, and/or to inhibit the lipogenesis in adipocytes, wherein the radicals R1 to R8, independently of one another, signify hydrogen, hydroxy or C1-C4-alkoxy, and/or two adjacent radicals together form a methylenedioxy group.
CA2250258C Novel tetralone or benzopyranone derivatives and process for producing the same The present invention provides new tetralone or benzopyranone derivatives and a method for producing the derivatives useful for a therapeutic agent for preventing and/or treating hormone dependent diseases. The present invention is a new tetralone or benzopyranone derivative represented by a particular general formula (I) (see formula I) wherein R1 represents a hydroxy group, an alkyloxy group or an aralkyloxy group, R2-R6 represent hydrogen, a hydroxy group, a straight or branched alkyloxy or aralkyloxy group having 1-6 carbon atoms, a halogen, an amino group or an alkylene dioxy group joined at R2 and R3, R3 and R4, R4 and R5, R5 and R6, and A represents a methylene or oxygen, but provided that when R1 is methoxy, R2-R6 are all hydrogens and A is the methylene. In the production, a particular tetralone or benzopyranone compound and a particular benzaldehyde compound are reacted.
WO2011068898A1 Protein kinase c inhibitors and uses thereof This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseThis disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.ases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
CN1593432A Alendronate sodium powder for injection Disclosed is an Alendronate sodium powder for injection which comprises the components of (by weight percentage), Alendronate sodium 0.125-100%, excipient 0-99.875%. The Alendronate sodium powder for injection can be used for treating high calcium blood disease caused by tumor or women's osteoporosis.
CN101129746A Bolus for relieving sore-throat and clearing throat The invention relates to a medicinal and dietary composition for treating throat pain, hoarseness, dry mouth and throat, difficult ingurgitation and preparing process, wherein the composition is prepared mainly from scrophularia root, root of ballon flower, mentha, sterculia seed, borax, subprostrate sophora root, goldthread root, honeysuckle flower and ophiopogon root, the medicament can also be used as a conventional health dietary preparation having no side effects but with easy administration.
EP2444089A2 Anhydrous compositions useful for attaining enhanced sexual wellness The invention relates to an anhydrous composition comprising a vasodilator and an acceptable carrier wherein the vasodilator is present in an amount effective to increase the blood flow when the composition is applied to human tissue. The compositions according to the invention are non-flushing.
EP2058313A2 Process for synthesis and purification of anhydrous crystalline S-zopiclone Process for synthesis and purification of anhydrous crystalline S-zopiclone for the preparation of enantiomerically pure {S)-5-{chloromethyloxycarbonyloxy)-6-{5-chloropyrid-2-yl)-7-oxo-5,6-dihydropyrrolo[3,4b]pyrazine (S)-(I).
CN101857542A Method for manufacturing low-lead granular zinc citrate The invention relates to a method for manufacturing low-lead granular zinc citrate, which is characterized in that: a raw material, namely zinc sulphate, is changed into soluble zinc sulphate solution, so that insoluble impurities in the zinc sulphate are more completely filtered out. However, the insoluble impurities cannot be separated out by the ordinary zinc oxide method and then are mixed in the final product. The steps of adding dilute acetic acid can effectively control the content of lead, so that the purity of the obtained zinc citrate is higher. The last step prevents the generation of dust in the production and the formation of particles. The problem on dust is solved.
CN101366709A Application of turmeric native The invention discloses novel application of a medicine - curcumin, namely application of the curcumin in preventing and treating or treating the Parkinson disease. After the curcumin acts on an MPTP-constructed Parkinson disease mouse model, the curcumin can effectively promote expression of tyrosine hydroxylase in substantia nigra, lighten damage of sneurotoxin on the tyrosine hydroxylase in substantia nigra, reduces damage of dopaminergic neurons, promote biosynthesis of damaged dopamine and promote restoration and growth of damaged dopaminergic neurons; the curcumin can also inhibit astrocytes to secrete gelatinous fiber proteins, reduce stimulus of the neurotoxin on the astrocytes and lighten phlegmonosis of a brain tissue; moreover, the curcumin can inhibit expression of induction type nitrous oxide synthase, lighten induction of the neurotoxin on the induction type nitrous oxide synthase and inhibit reinforcement of intracephalic oxidative stress reaction. Therefore, the curcumin can effectively reduce damage of the dopaminergic neurons, thereby having significant potential value in developing medicines for preventing and treating and/or treating the Parkinson disease.
WO2008013321A1 Novel sglt inhibitors Novel compounds of formula (A) or a pharmaceutically acceptable salt thereof: wherein symbols are as defined in claims, which are useful as SGLT inhibitors and for treatment of diabetes and related diseases.
CA2382599C Flushable disposable polymeric products Materials suitable for preparing components of flushable drug delivery systems are described. These components include drug impermeable and drug permeable materials, including materials that can be used to control the rate of release of drugs from the device, and pressure sensitive adhesive compositions which are drug compatible. Methods for fabricating these devices, including transdermal drug delivery patches, are described.
US6982263 Peptidyl carbamates; treatments for osteoporosis and autoimmune diseases Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.
CN101205244B Bimetallic heptanuclear anticancer compounds as well as preparation and uses thereof The invention relates to a bimetallic seven-nuclear anticancer compound and a preparation method as well as application thereof. The chemical formula of the bimetallic seven-nuclear anticancer compound is RE. Cu6(Mu-OH)3(Gly)6Im6Cl6; wherein, the rare earth ions RE in the bimetal are selected from La<3+>, Pr<3+>, Sm<3+>, Er<3+> or Nd<3+> and the metal copper ions are Cu<2+>; Gly symbolizes the glycine and Im symblizes the imidazole. The invention also provides the preparation method for compound and the application of the compound in the cancer cell inhibition. The bimetallic seven-nuclear anticancer compound of the invention has the advantages of simple preparation method, low price, strong anticancer capability and small drug dose, low toxicity, and environmental friendliness and has important application prospect at the aspect of metallic anticancer drugs.
CN101199646A External rubbing dose for treating psoriasis The invention discloses an external plaster to cure psoriasis prepared with the materials of 400-600 portions of medical cortex meliae, 400-600 portions of garden balsam herb, 1000-2000 portions of pepper, 400-600 portions of unbracteolated spurge root, 2500-3500 portions of cortex pseudolaricis, 400-600 portions of rumex madaio, 400-600 portions of rhododendron molle, 400-600 portions of chaulmoogra, 250-350 portions of centipede, 400-600 portions of asarum, 400-600 portions of angelica dahurica, 400-600 portions of semen momordicae, 400-600 portions of cynanchum paniculatum, 400-600 portions of cacumen platycladi, 100-1500 portions of cantharis, 500-3000 portions of borneol, 500-3000 portions of camphor, 500-3000 portions of peppermint ice, 2000-5000 portions of phenylformic acid, 300-1500 portions of gamboges, 300-4000 portions of clove oil, 300-1000 portions of tea plant oil, 9000-11000 portions of turpentine or pine tar, 500-40000 portions of cedar wood oil and a proper amount of alcohol with a concentration of 75%-95%. The ingredients supplement each other and act together, making the plaster good in curative effect. The plaster has no side effects after long-time use and is safe and has good effects in curing other diseases caused by ringworm.
US20120289592 Ercc1 gene expression level is associated with clinical outcomes in esophageal cancer patients The disclosure provides compositions and methods for identifying a cancer patient, such as an esophageal cancer patient, suitable for a therapy that includes administration of a platinum drug and radiation pre-operatively, based on the expression level of an ERCC1 gene. After determining if a patient is likely to be successfully treated, the disclosure also provides methods for treating the patients.
CN101317846B Tetrodotoxin formulation for drug rehabilitation , pain ease The present invention relates to a tetrodotoxin preparation used for drugs abstinence and analgesia. The preparation comprises small dose of tetrodotoxin that is taken as active ingredient of medicine and cosolvent or allowable supportting agent in pharmacy. The cosolvent is amino acid. In the present invention, the amino acid is taken as the cosolvent, which not only can act as the cosolvent forincreasing solubility of the tetrodotoxin in water, but also can form highly water-soluble salting liquid with the tetrodotoxin. The tetrodotoxin used in the present invention is prepared by adoptingthe specific method of the present invention. The purity of the prepared tetrodotoxin is as high as 98 percent with high yield. The preparation formed by the tetrodotoxin prepared by adopting the method provided in the present invention and amino acid is not only good in water solubility, but also good in stability, safe, reliable, stable in quality. The preparation does not need to be preserved in the refrigerator at specific temperature. The preparation can be preserved for more than 2 years at room temperature, thus greatly saving storage and transportation cost and providing convenience for use in medical treatment. The cure effect is evident, and in particular when applied to physiologic de-toxin, the tetrodotoxin preparation has a cure rate reaching 100 percent.
EP1494667A1 Imidazole compounds as anti-inflammatory and analgesic agents This invention provides a compound of the formula (1) wherein: R1 represents a hydrogen atom, an alkyl group, etc.; R2 represents a hydrogen atom, a halogen atom, etc.; R3 represents a hydrogen atom, an alkyl group, etc.; R4 represents an aryl group, etc.; A represents an aryl1, etc; B represents an alkylene etc.; X represents NH, etc.; or a phannaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of medical conditions mediated by prostaglandins such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
US20090155384 Methods and compositions for the sustained release of chromium Provided herein are compositions for the administration of chromium that include at least two components: a hydrophilic chromium complex and a lipophilic chromium complex, and methods of using the same. Also provided are compositions for the administration of chromium that include a first “fast-acting” chromium complex and a second “slow-acting” chromium complex, wherein the first chromium complex is absorbed more quickly than the slow-acting chromium complex, and methods of using the same. Also provided herein are methods for treating, preventing, and improving conditions associated with cardiometabolic syndrome, by identifying a subject in need of treatment, prevention, or improvement of a condition associated with cardiometabolic syndrome, and providing a therapeutically effective amount of a composition comprising a fast-acting chromium complex and a slow-acting chromium complex, to the individual.
WO2008045558A2 Benzothiadiazine compounds and their use Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and use thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukoc te accumulation are described hereia. R1 is NH2, -NHR2, OrNR4R5, where R4 and/or R5 are G1-6 aikyl; O3-Cg i, cycloaikyl; Cj-C8 heterocycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; or, R4 and. Rs, taken together with the nitrogen atom to which they are attached, form a heterocyclic or heteroaromatic ring; and provided that FU and R5 are hot both methyl;.
US20110142914 Inhalable compositions having enhanced bioavailability The present disclosure provides methods and compositions suitable for delivering lipophilic bioactive agents. The compositions may be utilized to treat numerous diseases and conditions that would benefit from the application of a lipophilic bioactive agent. In embodiments the compositions may be introduced by inhalation.
US20100298345 Synthetic compounds and derivatives as modulators of smoking or nicotine ingestion and lung cancer Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.
US20120065194 Use of cyproheptadine to treat organophosphate exposure A method of treating exposure to an organophosphate compound by administering a cyproheptadine compound to a subject in need thereof.
US7919614 Synthetic polysaccharides, process for their preparation and pharmaceutical compositions containing them Synthetic polysaccharides are disclosed containing 8-24 monosaccharide units made up of a concatenation of disaccharides consisting of a uronic acid and a hexose, wherein the hydroxyl groups of the polysaccharides are etherified with a C1-6 alkyl group or esterified in the form of a sulpho group, each disaccharide being at least monoetherified; and salts thereof, are disclosed.
CN103127208A Medicinal composition for treating chronic hepatopathy, and its application The invention discloses a medicinal composition for treating chronic hepatopathy. The medicinal composition is composed of astragaloside and glycyrrhizic acid, and the weight ratio of astragaloside to glycyrrhizic acid is 3-6:1. Results of tests and verification through adopting a classic animal model show that the medicinal composition can substantially reduce the collagen content of the hepatic tissue of a model rat, mitigate the hepatic fibrosis degree and the hepatic damage degree, improve the hepatic fibrosis resistance, effectively prevent the development of the hepatic fibrosis and promote the reversion of the hepatic fibrosis, the above effects are better than effects realized through singly using the above components, and the medicinal composition can be used for treating and preventing various diseases comprising chronic hepatitis, hepatic fibrosis, hepatic cirrhosis and the like. The medicinal composition can be processed to prepare oral solid preparations comprising a tablet, a granule, a capsule and the like.
CN101735217B Application of imidazole [4,5-f][1,10] phenanthroline and derivative thereof to preparation of antineoplastic drug The invention discloses an application of an imidazole [4,5-f][1,10] phenanthroline and a derivative thereof to the preparation of an antineoplastic drug. The structural formula of the imidazole [4,5-f][1,10] phenanthroline is as shown in formula I: wherein R is selected from components of hydrogen, C1-6 alkyl or C1-6 substituted alkyl, phenyl or substituted phenyl, pyridyl or substituted pyridyl, furyl or substituted furyl, pyrrolyl or substituted pyrrolyl, or thiazolyl or substituted thiazolyl. The imidazole [4,5-f][1,10] phenanthroline and the derivative thereof are used for preparing the antineoplastic drug and have remarkable inhibiting effect on tumor cells.
US7214697 2-Oxo-benzimidazolyl substituted ethanolamine derivatives and their use as β3 agonists The present invention relates to a β3 adrenergic receptor agonist of formula (I), wherein R is C3–C8 alkyl or (C3–C7 cycloalkyl)C1–C5 alk-di-yl: R1 is H, CN, halo; C1–C6 alkyl, C1–C4 haloalkyl, CO2 R6, CONR6R6, NR6COR7, NR6R6, OR6, SR6, SOR7, S02R7 or SO2NR6R6; R1a is H, halo or C1–C6 alkyl; R2 is H or C1–C6 alkyl; R3 and R4 are independently H or C1–C6 alkyl R5 is hydrogen, optionally substituted phenyl or optionally substituted heterocycle; X is absent or is OCH2 or SCH2; X1 is absent or C1–C5 alk-di-yl; and X2 is absent or is O, S, NH, NHSO2, SO2NH or CH2; or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity
CA2382919C Bicyclic imidazo-3-yl-amine derivatives The invention relates to bicyclic imidazo-3-yl-amines of general formula (I) provided in the form of bases or of pharmaceutically acceptable salts thereof. The invention also relates to methods for producing the inventive bicyclic imidazo-3-yl--amines and to medicaments containing, as an active ingredient, at least one imidazo-3-yl-amine of general formula (I) that is provided in the form of the base or of a pharmaceutically acceptable salt.
CN102335153A Piperazine ferulate sustained-release tablet and its preparation method The invention describes a piperazine ferulate sustained-release tablet and its preparation method. The piperazine ferulate sustained-release tablet consists of piperazine ferulate, a framework material, a diluent, a lubricant, an adhesive, and optionally a coating material. In the invention, starch1500 (shanda in Chinese) is added into the diluent to improve the release of the sustained-release preparations. Meanwhile, a strict preparation process is employed so as to make the tablet of the invention reach a release result approximate to human in vivo release. With simple analysis of dissolution and release, the tablet and its preparation method are suitable for large scale production. According to a rotating basket method for in vitro drug release of sustained-release preparations in the 2010 edition of Chinese pharmacopoeia, in 900ml of water, the release rate of the tablet in the invention can be 25-35% accumulatively in 2h, 45-60% in 4h, 60-75% in 6h, and over 90% in 12h. A detailed study of the in vitro release result of the tablet indicates that the piperazine ferulate sustained-release tablet reaches good sustained-release effects and can have delayed release within 12h, so that the medicine taking time can be reduced.
WO2014028801A1 Cyclopentylpyrazoles as n-type calcium channel blockers Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, Q, and G are defined herein.
CN102718817A Method for preparing anthocyanin extract from black bean peel The present invention relates to a method for preparing an anthocyanin extract from black bean peel and solves the problem that existing extracts have low effective component content and high protein content. The method comprises the following steps of: firstly extracting black bean peel by the use of an acidic solvent, condensing the extracted solution, removing the solvent, adding acidic protease for enzymolysis, absorbing the enzymolysis solution by the use of resin, carrying out desorption and elution on the adsorbent resin, condensing and drying the elution solution after desorption, so as to obtain the protein-free anthocyanin extract. In addition, studies show that the protein-free anthocyanin extract and a standard extract of Ginkgo biloba have antioxidant anti-aging synergy.
US7285558 Helicobacter infections; bactericides Compounds having the general formula and pharmaceutical compositions containing them, and their use in the treatment or prophylaxis of H. pylori infection.
CN102702451A High-efficiency and antibacterial polymeric micelle with high pH sensibility and biocompatibility and preparation method thereof The invention belongs to the field of macromolecular nano biological medicine materials, and in particular relates to a high-efficiency and antibacterial polymeric micelle with high pH sensibility and biocompatibility and a preparation method thereof. An amphipathic block polymer is subjected to self-assembly by a direct dissolution method to form the micelle; and the surface of the micelle has a large number of positive charges, so that the micelle has the effects of sterilizing and inhibiting bacteria in high efficiency under the condition that other antibiotics are not added. Simultaneously, the micelle has high biocompatibility and biodegradability. The polymeric micelle has high pH sensibility, and a structure of the polymeric micelle is changed with the change of the outside pH value, and multiple medicines can be wrapped by a core-shell structure of the micelle, so the polymeric micelle has a bright application prospect.
US20110003010 Phosphoric Acid Esters Containing Phosphorus Atoms Bridged By Diol Units Phosphoric esters comprise A) one or more structural units derived from substances of component a), the substances of component a) being selected from orthophosphoric acid and one or more of its derivatives, B) one or more structural units derived from substances of component b), the substances of component b) being selected from one or more compounds of formula (I) R2—O—(CH2CH2O)u(C3H6O)v(DO)w—H (I) and C) one or more structural units derived from substances of component c), the substances of component c) being selected from one or more diols of formula (II) HO—(CH2CH2O)a(C3H6O)b(DO)c—H (II) where the sum total a+b+c is ≧1 and the phosphoric ester contains 2 or more phosphorus atoms per molecule which are bridged via a structural unit derived from the compounds of formula (II). The phosphoric esters of the invention are very useful in the manufacture of cosmetic, pharmaceutical and dermatological compositions.
CN1861081A Use of phytolaccatoxin for preparing medicine to treat mazoplasia An application of phytolaccatoxin A with the chemical formula: 3-0-(beta-D- glucopyranose-beta-D-xylopyranose)-2-hydroxy phytolaccic acid-30-methyl ester in preparing the orally taken or exterior-applied medicines for preventing and treating mastoplasia is disclosed.
US7449585 1,2-dihydro-2-(4-trifluoromethylphenyl)-6-(3-trifluoromethyl-2-pyridinyl)-3H-indazol-3-one; capsaicin receptor ; analgesic, antiinflammatory, hypotensive agent; rheumatoid arthritis, osteoarthritis, headache, migraine, cancer and central nervous system pain, irritable bowel syndrome Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
CN103421003A Coptisine derivatives with lipid regulation and hypoglycemic functions The invention provides coptisine derivatives with lipid regulation and hypoglycemic functions, physiologically acceptable salt of the coptisine derivatives, solvates, a preparation method and medicine compositions containing the compounds. The result of cell glucose consumption experiments shows that the compounds have functions of promoting glucose consumption. The result of animal experiments shows that the compounds can reduce the total cholesterol level in serum of hyperlipidemia model golden hamsters obviously. The compounds can be used for preventing and treating metabolic syndrome.
US20110160129 Therapeutic Agent Preparations for Delivery Into a Lumen of the Intestinal Tract Using a Swallowable Drug Delivery Device Embodiments of the invention provide swallowable devices, preparations and methods for delivering drugs and other therapeutic agents within the GI tract. Many embodiments provide a swallowable device for delivering the agents. Particular embodiments provide a swallowable device such as a capsule for delivering drugs into the intestinal wall or other GI lumen. Embodiments also provide various drug preparations that are configured to be contained within the capsule, advanced from the capsule into the intestinal wall and degrade within the wall to release the drug to produce a therapeutic effect. The preparation can be coupled to an actuator having a first configuration where the preparation is contained in the capsule and a second configuration where the preparation is advanced out of the capsule into the intestinal wall. Embodiments of the invention are particularly useful for the delivery of drugs which are poorly absorbed, tolerated and/or degraded within the GI tract.
EP2366702A1 New oxadiazole derivatives The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or N-oxide thereof: and its use in the treatment of diseases which are susceptible to improvement by sphingosine-1-phosphate (S1P1) receptor agonists.
CN103127117A Pharmaceutical composition of levodopa/benserazide/folic acid compounds and purpose thereof The invention relates to a pharmaceutical composition of levodopa/benserazide/folic acid compounds and a purpose thereof, and belongs to the technical field of pharmacy. The pharmaceutical composition comprises the levodopa with medical dose, the benserazide with the medical dose, the folic acid compounds with the medical dose and a carrier which can be accepted in the pharmacy. The dose of the levodopa is 100-300 mg, the dose of the benserazide is 30-70 mg, and the dose of the folic acid compounds is 0.2-1.6 mg. The pharmaceutical composition of the levodopa/the benserazide/the folic acid compounds and the purpose thereof have the advantages of enhancing the curative effect of Parkinson disease resistance and improving the quality of life of a patient through the synergistic effect of multiple target points; being capable of effectively preventing and lowering the occurring risk of cerebral apoplexy of a Parkinson disease patient through a homocysteine (Hcy) target point; and in addition, enabling the patient to take medicine conveniently.
CN101912401A Compound cefalexin capsule and preparation method thereof The invention belongs to the field of broad-spectrum antibiotics, in particular to a compound cefalexin capsule and a preparation method thereof. The compound cefalexin capsule contains 225-275 mg of cefalexin and 3.6-4.4 mg of bromhexine hydrochloride. The compound cefalexin capsule provided in the invention has the advantages of reasonable formula, high drug dissolution, simple preparation process and less pollution.
US20110104301 Methods of reducing pain and inflammation Provided herein are methods of treating or preventing pain and/or inflammation in a subject comprising administering to the subject a transient receptor potential (TRP) ion channel inhibitor.
CN102349887A Diclofenac sodium acetaminophen gastrointestinal type capsule medicinal composition The invention provides a diclofenac sodium acetaminophen gastrointestinal type capsule medicinal composition, which can overcome the defects in the prior art, and effectively solve the problems of the stability, clinical medicinal safety and the like of a diclofenac sodium and acetaminophen compound, fulfill the aim of absorbing diclofenac sodium and acetaminophen by different parts simultaneously and play a good synergistic treatment effect. By the screening and optimization of a formula, the diclofenac sodium acetaminophen gastrointestinal type capsule medicinal composition is provided, and the preparation ensures the stability of medicines in the production and storage processes. In addition, the invention provides a preparation method for the medicinal composition, and the method is simple and feasible, and is suitable for large-scale industrial production by pilot-plant enlargement.
CN102836131A Sustained release microsphere preparation for hypodermic injection of buprenorphine and preparation method thereof The invention discloses a sustained release microsphere preparation for hypodermic injection of buprenorphine and a preparation method thereof. The sustained release microsphere preparation comprises 0.01-1 percent by mass of buprenorphine and 50-99.99 percent by mass of biodegradable medicinal high polymer material counted by the weight of microspheres. The sustained release microsphere preparation can be prepared by adopting a multi-emulsion method, a water-free method, a low-temperature spray extraction method, a method for preparing into nanoparticles and coating into a microsphere preparation, a phase agglomeration method and the like. The sustained release microsphere preparation can be released continuously for about 15 days, 30 days or 60 days in vitro, and can be released continuously for at least 30 days in a rat; and due to the adoption of the sustained release microsphere preparation, the administration times are reduced, the bioavailability is enhanced, the toxic and side effects on a whole body are reduced, and the compliance of a patient is improved.
US20110117094 Reactivation of Axon Growth and Recovery in Chronic Spinal Cord Injury Disclosed are methods of treating chronic nervous system diseases or injuries, e.g., chronic spinal cord injury, using Nogo receptor antagonists, including Nogo receptor-1 (NgR1) polypeptides, Nogo receptor-1 antibodies and antigen-binding fragments thereof, soluble Nogo receptors and fusion proteins thereof, and polynucleotides. Also disclosed are methods of noninvasively monitoring axonal growth during and after treatment with an axonal growth promoting agent.
EP1515607A2 Antimicrobial compositions, products and methods employing same Antimicrobial compositions that provide enhanced immediate and residual anti-viral and antibacterial efficacy against rhinovirus, rotavirus, Gram-positive bacteria, Gram-negative bacteria and combinations thereof. More specifically, antimicrobial compositions comprising an organic acid or organic acid mixture and a short-chain anionic surfactant having at least one of a large head group; a branched alkyl chain and an unsaturated alkyl chain. Further, products incorporating the antimicrobial compositions of the present invention and methods of using the antimicrobial compositions and products disclosed herein.
WO2013009102A3 Cartilage cell treating agent comprising collagen, hyaluronic acid derivative, and stem cell derived from mammal umbilical cord The present invention relates to a medical composite biomaterial. More specifically, the present invention relates to the medical composite biomaterial comprising collagen and a hyaluronic acid derivative. Also, the present invention relates to a cartilage cell treating agent using the biomaterial and stem cells derived from a mammal umbilical cord. The biomaterial does not cause an immune system reaction, has superior durability, and the cartilage cell treating agent comprising the biomaterial and the stem cells enables arthroscopic surgery, thereby reducing pain of the patient, and can effectively treat degenerative arthritis and cartilage damage.
EP1856259A1 Rnai-mediated inhibition of frizzled related protein-1 for treatment of glaucoma RNA interference is provided for inhibition of Frizzled Related Protein-1 mRNA expression, in particular, for treating patients having glaucoma or at risk of developing glaucoma.
CN101411734A Method for treating hyperosteogeny The invention relates to a method for treating hyperosteogeny. The method is characterized in that a medicine comprises the following compositions in mass portion: 6 to 10 portions of rhizoma ligustici wallichi, 10 to 30 portions of Shanxi mature vinegar and 1 to 1.5 portions of medicinal vaseline. A manufacturing method comprise the following steps: the rhizoma ligustici wallichi is pulverized to form powders, is added with the Shanxi mature vinegar, is stirred to a paste, is mixed with the medicinal vaseline and is evenly mixed; subsequently, prepared ointment is applied on the hyperplasia part of a patient; after application, one layer of plastic paper is covered on the ointment; a gauze is stuck on the plastic paper; and the periphery of the gauze is fixedly sealed through wide adhesive plaster. The medicine is matched for use and has the effects of activating blood and relieving pain and has special effect in treating hyperosteogeny and no poor reaction.
EP1003370B1 Method of enhancing magnesium absorption and prevention of atherosclerosis A method for making and administering a compounded coordination complex of magnesium that enchances the biological absorption of an effective amount of potentiated magnesium, and when administered in therapeutically effective dosages balances calcium metabolism, maintains the homeostasis of the cardiovascular system, and prevents atherosclerosis in the human body.
US20060246046 Modified tridegins, production and use thereof as transglutaminase inihibitors The invention relates to modified tridegins, polypeptides derived from SEQ ID No. 1, in which the modification is replacement of a cysteine residue and/or one of the following amino acids—Lys2, Lys7, His10, Gly12, Leu24, Tyr31, Phe34, Arg39, Ile45, Met48, Asp50, Pro55, Phe58, Asn60, Pro65, Arg66, by another amino acid and/or N- or C-terminal deletion, whereby the remaining polypeptide comprises at least the amino acid sequence DDIYQRXVXFPXLPL (SEQ ID NO.89) and/or a covalent bonding to polyethylene glycol. Said polypeptides are novel inhibitors of transglutaminases, in particular of Factor XIIIa, of the terminal enzymes in the blood coagulation cascade. The invention further relates to methods for production of said inhibitors and the use thereof as transglutaminase inhibitors.
CN1887293A Slimming composition with cross-linked monosaccharide/disaccharide and dietary fiber The present invention relates to cross-linked monosaccharide/disaccharide compositions with or without diet fiber medicine and/or health article, slimming or hypolipidemic medicine and/or health article. The cross-linked monosaccharide/disaccharide compositions have cross-linking agent with functional group capable of cross-linking with hydroxyl group. The present invention also relates to the preparation of these cross-linked monosaccharide/disaccharide compositions. The compositions of the present invention may be prepared in industrial scale, and the present invention expands the application range of monosaccharide and disaccharide.
EP1347805B1 Pharmaceutical preparation for douches and/or irrigations of natural or pathological cavities in the human body A preparation for douches and/or irrigations of natural or pathological cavities in the human body which comprises water added with at least one gaseous substance selected from carbon dioxide, oxygen, nitrogen, gaseous anaesthetic substances and inert gases.
EP2405972A1 Use of rosuvastatin lactols as medicaments This invention relates to the discovery of novel rosuvastatin analogues. More specifically, the invention relates to novel rosuvastatin analogues which have utility in treating conditions treatable by the inhibition of HMG-CoA reductase.
US6855698 Topoisomerase I selective cytotoxic sugar derivatives of indolopyrrolocarbazoles The present invention relates to fluoro sugar and other sugar derivatives of indolopyrrolocarbazoles, their salts and hydrates, which exhibit selective topoisomerase I (topo I) activity, are useful in inhibiting the proliferation of tumor cells and exhibit an antitumor effect, as well as processes for their preparation.
CN102552297A Application of medicinal composition to preparation of alpha-glucuroide inhibitor medicines The invention discloses new application of a medicinal composition extracted from Cortex Ilicis Routundae to preparation of alpha-glucuroide inhibitor medicines. The medicinal composition is characterized by comprising substances such as syringin, rotundic acid and the like; the alpha-glucuroide inhibitor medicines may be a composition which consists of the syringin and the rotundic acid or preparations which are prepared from the composition which consists of the syringin and the rotundic acid and other medicines; and the medicinal composition can be prepared into tablets, capsules, granules, injection and suspensions.
WO2009075841A2 Methods of using (+)-1,4-dihydro-7-[(3s,4s)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid for treatment of antecedent hematologic disorders Methods of treating, preventing or managing antecedent hematologic disorders, such as myelodysplastic syndrome, including chronic myelomonocytic leukemia are disclosed. The methods encompass the administration of SNS-595. Also provided are methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. In certain embodiments, the method of treatment comprise administering SNS-595 in combination with cytarabine. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed.
CN101317982A Method for preparing capsule for cooling liver, removing wind, clearing heat and relieving spasm The present invention discloses a method for producing a capsule for cooling the liver, stopping wind, clearing heat and relieving muscular spasm. The method includes the following procedures: refining twenty medicinal materials of gastrodia tuber, hooked uncaria, parasite scurrula, achyranthes root, eucommia, motherwort, pachyma cocos, radix pittospuri, baical skullcap, sea-ear shell, multiflower knotweed, antelopes horn powder, white muscardine silkworm, heliconia, arsenic sulphide, chilopod, tabasheer, amber, vermilion, musky oyster, raw Hangzhou peony, bllackened swallowwort root, dwarf lilyturf , medicinal cyathula toot, rehmannia root, figwort root, radix pittospuri, bamboo shavings, green orange leaf, fried orange fruit and liquorice; preparing medicinal materials into dry powder and proportionally mixing the dry powder with stearic acid magnesium; taking ethanol as the moisturizing agent and preparing mixture into particles; drying and capsulizing the particles to obtain the capsule. The medicine of the present invention has the characteristics of simple and clear composition, advanced technique, easy quality control, high technological content, convenient use for patients, good taste, difficult moist absorption and good stability; the capsule is characterized by high biological utilization and equal curative effect with other dosage forms. The preparation with reasonable design, convenient use and convenient carry has the unique curative effect of cooling the liver, stopping wind, clearing heat and relieving muscular spasm.
CN101401792B Method for preparing nanocapsule and nanocapsule composite microsphere The invention discloses a method for preparing a nanometer capsule and a method for preparing a nanometer capsule composite microsphere. The method for preparing the nanometer capsule comprises the following: step 1, preparing a methotrexate alkaline solution and a PLGA-CH2Cl2 solution; step 2, injecting the methotrexate alkaline solution into the PLGA-CH2Cl2 solution to obtain a W/O colostrum after ultrasonic emulsification; step 3, adding the colostrum into sodium cholate to obtain a W/O/W multiple emulsion after the ultrasonic emulsification; and step 4, placing the obtained multiple emulsion in the sodium cholate to be evaporated through decompression to remove CH2Cl2 so as to obtain a nanometer capsule particle suspension. The method for preparing the nanometer capsule composite microsphere comprises the following: step a, preparing a nanometer capsule; and step b, preparing the nanometer capsule composite microsphere. The nanometer capsule particle prepared by the invention has the characteristics of even size, higher drug loading and encapsulation efficiency, peak value drug release, and smooth drug release.
CA2855932A1 Pkc activators and combinations thereof The present disclosure relates to PKC activators and combinations thereof. The disclosure further relates to compositions, kits, uses, and methods thereof.
CA2242878C Induction of immune response against desired determinants The present invention provides compositions and methods of inducing immune response in patients. In particular, it provides compositions useful in inducing humoral responses against desired immunogens, particularly polysaccharides.
EP2550964A1 Temsirolimus for use in the prevention and/or treatment of a delta 9-tetrahydrocannabinol-induced anxiety disorder The invention relates to temsirolimus for use as a medicament to prevent and/or treat a Δ9-tetrahydrocannabinol-induced anxiety disorder and to compositions comprising both agents.
CN101220360A SiRNA sequence restraining caspase-3 gene expression The invention relates to a siRNA double-strand sequence, which is a siRNA sequence for inhibiting caspase-3 gene expression. The invention solves the problem that the prior art has no siRNA sequence which is most appropriate for inhibiting the caspase-3 gene expression, the sequence is siRNA1: a sense strand is 5'-GGGAAACAUUCAGAAACUUtt-3' and an antisense strand is 5'-AAGUUUCUGAAUGUUUCCCtg-3'; the siRNA double-strand sequence which is provided by the invention can be used for preparing drugs for inhibiting neural cell apoptosis or treating neurodegenerative diseases. The siRNA double-strand sequence enters into a biosome in a certain mode, which is the specific expression for inhibiting the disease-related proteins and is more effective than any means; the invention can lead related disease genes to be in silence, carry out effective knockout to the expression of a target gene and achieve treatment purpose, and the specificity of the sequence and the powerful effect of the gene inhibition effect are unbeatable compared with the other drugs.
CN103385883A Pharmaceutical composition containing tropisetron hydrochloride and fructose The invention relates to a pharmaceutical composition containing a tropisetron hydrochloride injection and a fructose injection, and particularly relates to a composite application package comprising the tropisetron hydrochloride injection and the fructose injection. In use, the tropisetron hydrochloride injection is dissolved into the fructose injection, and then the mixture is used for intravenous infusion. The pharmaceutical composition containing the tropisetron hydrochloride injection and the fructose injection has the effect of treating postoperative nausea and emesis, and also is capable of replenishing energy and body fluid of human body.
CN103142624A Application of antibiotic tigecycline in preparing anti-cancer medicine The invention discloses a new function of antibiotic tigecycline, namely an anti-cancer function of antibiotic tigecycline. Through an experiment, the inventor finds that tigecycline (TIG) can inhibit the growth of gastric cancer cell line MKN-45 and gastric cancer low-passage cell GAM-016; the TIG can block the cell cycle of the gastric cancer cell line MKN-45 and the gastric cancer low-passage cell GAM-016; the TIG can promote the autophagy of the gastric cancer cell line MKN-45 and the gastric cancer low-passage cell GAM-016; and the TIG has a function of inhibiting gastric cancer growth on a mice-with-tumor model of gastric cancer.
CN102614108A Cubic water quality liquid crystal gel transdermic absorption preparation containing oxybutynin chloride and preparing method thereof The invention discloses a cubic water quality liquid crystal gel transdermic absorption preparation containing oxybutynin chloride and a preparing method thereof. The preparation contains the following components by weight percentage with the total weight of the preparation as standard: 1%-30% of oxybutynin hydrochloride or basic group of oxybutynin hydrochloride, 13%-90% of solvent, 0.1%-20% of gel host material, 23%-90% of solvent, 0.2%-30% of oily permeating skin penetration enhancer, 0.1%-35% of liquid crystal gel emulsifier, 1%-60% of water and 0.01%-15% of potential of hydrogen (pH) regulator. The preparation has better efficiency performance, can reduce medicine taking frequency, improves adaptability of users, simultaneously avoids first-pass effect when medicine is orally takenand passes through gastrointestinal tract and liver due to skin permeating method, and has higher bioavailability.
US7521458 Spiropiperidylrifamycins for the treatment of mycobacterial infections The compounds of formula (1), their pharmaceutically acceptable salts and their solvates, wherein R1 is a radical selected between hydrogen and alkyl; R2 is selected from hydroxyalkyl, phenyl, phenyl mono-substituted and phenyl di-substituted in positions 3 and 4; R3 is selected from phenyl, phenyl mono-substituted and phenyl di-substituted in positions 3 and 4; the substituents of the phenyl of R2 and R3 selected from halogen, (C1-C4)-alkyl and (C1-C4)-alkoxyl and R4 is selected from hydrogen, alkyl allyl and homoallyl, they are useful for the treatment of mycobacterial infections, in particular for the treatment of infections produced by Mycobacterium tuberculosis, Mycobacterium avium-intracellulare complex or Mycobacterium kansasii.
US20100143416 Alpha-defensins as anthrax immunotherapeutis The present invention relates to the use of an alpha-defensin in the manufacture of a medicament for the treatment, amelioration or prevention of a disease caused by Bacillus anthracis (B anthracis) infection. Furthermore, methods for the treatment of an B. anthracis infection as well as methods of protection against a B. anthracis infection, e.g. a vaccination are described.
EP0758890B1 Use of no scavengers, inhibitors or antagonists in the treatment of migraine Use of a NO scavenger or an inhibitor or antagonist for the production of a pharmaceutical composition for the treatment of migraine or other vascular headaches is described, as well as a method for the treatment of migraine or other vascular headaches in mammals, which comprises administering to said mammal an effective amount for said treatment of a NO scavenger or a specific inhibitor or antagonist. The active principle is desirably a NO synthase inhibitor, preferably L-NMMA.
CN103536615A Preparation method of didymin and isosakuranetin, and application thereof in anti-diabetic medicine The invention belongs to the technical field of pharmacy, and discloses application of didymin and isosakuranetin in preparation of an anti-diabetic medicine and a preparation method. The didymin and the isosakuranetin are separated from a calamint (Clinopodium.chinese (Benth.)O.Kuntze) herb; a concentrated extract is obtained from the calamint herb after the process of drying, crushing, alcohol extraction, and reduced pressure recovery; an ethyl acetate extract is obtained after alkali-solution and acid-isolation and ethyl acetate extraction; the didymin and the isosakuranetin are obtained from macroporous resin, polyamide and silica gel in manners of gel column chromatography and recrystallization; the didymin and the isosakuranetin have the effects of significantly reducing blood sugar of mice with alloxan diabetes, reducing serum total cholesterol, and improving vascular endothelial cell insulin resistance caused by free fatty acid and injuries on vascular endothelial cells caused by high glucose. The didymin and the isosakuranetin can be applied to prevention and treatment of cardiovascular and cerebrovascular diseases such as diabetes mellitus, dyslipidemia caused by the diabetes mellitus, a coronary heart disease, atherosclerosis and the like, and diabetic peripheral vasculopathy.
CN100577176C Extractive of Chinese globeflower in short petal, effective content of anti inflammation and usage An extract of short-petal garden nasturtium its anti-inflammatory component, its extracting process, the separating and purifying process of its active components, its composite medicine, and its application in preparing anti-inflammator medicines for treating rheumatic or rheumatoid arthritis are disclosed.
US20090263500 Composition and method for treating bedsores, cuts and burns The invention provides a composition and method to prevent and treat bedsores rapidly, efficaciously and economically. The composition comprises a novel combination of herbal extracts that has surprisingly synergistic and highly efficacious effects for the acceleration of wound healing, and which also disinfects and relieves pain in dermal wounds. The composition can also be used for the rapid healing of dermal burns and dermal cuts. The composition is comprised of extracts of aloe vera, passion flower, goldenseal, and American ginseng, and optionally includes ionic silver and mimosa extract. The treatment method comprises administering a fluid and or gel form of the composition to the wounded skin and or wound cavity therein as a prophylactic or therapeutic dose, and may be delivered by means of a wound dressing.
WO2011079230A2 Heterocyclic compounds as janus kinase inhibitors The invention provides compounds of formula (I): (Formula (I)), or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula (I).
CN1742729A Rifampicin medicine and preparing method The preparation method of rifampicin injection includes the following steps: slowly adding 300g of rifampicin into 1000ml of mixed solution under the condition of continuously stirring, said mixed solution is made up by mixing (by volume ratio) 0.75-1.2% of chemical inhibitor anhydrous sodium sulfite, 0.01-0.05% of metal ion complexing agent disodium ethylene diamine tetraacetate and 98.75-99.2% of organic solvent propylene alcohol, stirring them for 10-20 min, slowly drop-adding 5% NaOH under the condition of stirring, regulating pH to 6.5-9.0, adding active carbon for injection, stirring for 10 min, filtering to remove carbon, filtering by means of microporous filtering film, making constant volume to 5000ml, filling into glass ampule, charging nitrogen gas, sealing, sterilizing for 30 min by means of flowing steam with 100deg,C. cooling, checking and packaging.
US20120070452 Immunoadjuvant composition and use thereof Disclosed is a composition comprising, as an active ingredient, at least one selected from the group consisting of a Zc3h12a gene inhibitor and a Zc3h12a protein inhibitor. This composition can be used as an immunoadjuvant.
US6992084 Compounds and methods for modulating CXCR3 function The invention provides compounds and compositions of the formula: wherein, the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl, R1 is a member selected from the group consisting of substituted or unsubstituted (C5–C15)alkyl and (C8–C14)acyl group; R2 is a member selected from the group consisting of substituted or unsubstituted (C1–C8)alkyl; each R3 is independently a substituent Y is a member selected from the group consisting of substituted or unsubstituted (C2–C8)alkylene and substituted or unsubstituted (C2–C8)heteroalkylene; Z is —NR4R5 R4 and R5 are independently selected from the group consisting of hydrogen and (C1–C8)alkyl or taken together with the nitrogen atom to which each is attached to form a heterocyclyl or heteroaryl; These compounds and compositions bind to the CXCR3 chemokine receptor and are useful for treating diseases and conditions responsive to the modulation of CXCR3 activity, such as multiple sclerosis, rheumatoid arthritis, psoriasis, cancer, infectious disease, angiogenesis, and graft rejection.
US20080269272 Anticancer agents; psoriasis; prevent activation of hedgehog gene passageways The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.
EP2558086A1 Homeopathic medicament comprising phenacetin for the treatment of cancer The present invention relates to a composition comprising phenacetin, in particular a Phenacetinum 4CH homeopathic medicament for the use in the treatment of cancer.
WO2006063526A1 Use of cymipristone for treating depression The invention relates to the use of cymipristone compounds of formula (I) or pharmaceutically acceptable salt or isomer thereof in preparation of medicines for treating depression, especially major depression, more especially psychotic major depression; as well as a pharmaceutical composition for treating depression, especially major depression, more especially psychotic major depression comprising compounds of formula (I) or pharmaceutically acceptable salts or isomers thereof.
CN1980908A Substituted thiazoleacetic as CRTH2 ligands Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is -S-, -O-, -N=N-. -NR7-, -CR7=CR8-, -CR7=N-, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group -COOH, or a carboxyl bioisostere; rings Ar<2> and Ar<3> each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar<2> and Ar<3>, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.
CN102631365A Medicine composition containing mecobalamine The invention relates to a medicine composition containing mecobalamine, which is prepared from mecobalamine, retinoic acid and a pharmaceutic adjuvant, wherein the pharmaceutic adjuvant comprises a filling agent and an adhesive, the filling agent is selected from one or more of starch, pregelatinized starch, lactose, powdered sugar, mannitol, dextrin, microcrystalline cellulose and sucrose, and the adhesive is a 40-60 percent alcohol solution. The medicine composition has the inhibition rate of reaching 60 percent to the growth of a G422 brain glioma strain.
US20110020429 Use of particles comprising an alcohol Novel use of ultrasound sensitive drug carrying particles comprising an alcohol is disclosed, as well as products and methods thereof. The drug carrying particles accumulate in the diseased target tissue and efficiently release their payload upon ultrasound exposure.
US20100233286 Preparations of suspensions A method for preparing a suspension of LDH particles comprises the steps of preparing LDH precipitates by coprecipitation to form a mixture of LDH precipitates and solution; separating the LDH precipitates from the solution; washing the LDH precipitates to remove residual ions; mixing the LDH precipitates with water; and subjecting the mixture of LDH particles and water from step (d) to a hydrothermal treatment step by heating to a temperature of from greater than 80° C. to 150° C. for a period of about 1 hour to about 144 hours to form a well dispersed suspension of LDH particles in water.
CN1810809A Coumarether compound and new use of its composition The present invention discloses one kind of coumar ether compound extracted from feverfew or its pharmaceutically acceptable salt, and the application of the coumar ether compound or its pharmaceutically acceptable salt, the extract containing the coumar ether compound or its pharmaceutically acceptable salt and their medicine composition in treating bronchial asthma, bronchitis and emphysema. Animal experiment shows that the coumar ether compound extracted from feverfew can treating bronchial asthma, bronchitis and emphysema effectively.
DE202006002547U1 Combination, useful for preventing short term memory loss, confusion disease and Alzheimer's dementia, comprises potassium, alkaloids and medicament water Combination for preventing e.g. short-term memory loss and confusion disease, comprises potassium, alkaloids and medicament water. - ACTIVITY : Nootropic; Neuroprotective. - MECHANISM OF ACTION : None given.
CN103211777A Pharmaceutic preparation of duloxetine hydrochloride and preparation method thereof The invention belongs to the technical field of medicines, and in particular relates to a preparation method of duloxetine hydrochloride enteric coated drugs. The duloxetine hydrochloride is prepared by wrapping four layers of coating on a blank mini-pill, wherein the four layers of coatings are respectively a drug carrier layer, an isolation layer, a enteric coating layer and a film coating layer.
CN103638185A Medicine for treating odontalgia The invention relates to a medicine for treating odontalgia. Every dose is composed of 60g of radix rehmanniae, 24g of cortex moutan, 60g of gypsum, 24g of green tangerine orange peel, 18g of herba schizonepetae and 18g of radix sileris. The preparation and application method comprises the following steps: decocting in water twice, uniformly mixing the two decoctions, and taking by four times and 1 dose a day, wherein the dosage is reduced for children according to condotions. In the medicine taking period, oily, greasy, hot and spicy food is forbidden. The medicine solves the problem of great side effect in the existing medicine for treating odontalgia, and is suitable for treating odontalgia.
CA2725425A1 Homocysteine synthase inhibitor The present invention aims to provide a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving,homocysteine synthase. The present invention relates to use of a compound represented by the following formula (I) (see formula I) wherein each symbol is as defined in the DESCRIPTION, or a pharmacologically acceptable salt thereof, or a solvate thereof as a homocysteine synthase inhibitor.
US20130035367 Antisense oligonucleotides that target a cryptic splice site in ush1c as a therapeutic for usher syndrome The present invention provides a method for treating Usher's syndrome in a human subject including administering to the human subject an oligonucleotide having 8 to 30 linked nucleosides having a nucleobase sequence comprising a complementary region comprising at least 8 contiguous nucleobases complementary to a target region of equal length within exon 3 of an Usher RNA transcript.
WO2006057901A3 2-METHYLENE-19-NOR-1α-HYDROXY-17-ENE-HOMOPREGNACALCIFEROL AND ITS USES This invention discloses 2-methylene-19-nor-17-ene vitamin D analogs, and specifically 2-methylene-19-nor-1α-hydroxy-17-ene-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat aut6oimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment of obesity.
US20120071461 Substituted Benzamide Compounds Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
CN102018720A Preparation method of vitamin complex freeze-dried powder injection The invention discloses a preparation method of a vitamin complex freeze-dried powder injection. The method comprises the following steps of: weighing 12 types of vitamins; adding a part of principle medicaments into polysorbate 80, stirring for dissolving, adding 40 percent water for injection and stirring for dissolving; adding the remaining principle medicaments into the solution, stirring for dissolving and replenishing water for injection to 80 percent of the total amount of the water for injection; measuring the pH of the solution and filtering by using a filter membrane; pre-freezing, namely, lowering the temperature of the injection to 15 DEG C below zero and oscillating and refrigerating at the temperature of between 6 DEG C below zero and 15 DEG C below zero; lowering the temperature to 33 DEG C below zero and 35 DEG C below zero and oscillating and refrigerating at the temperature of between 25 DEG C below zero and 35 DEG C below zero for 40 to 60 minutes; performing sublimation drying; drying once again; and gradually raising the temperature of a medicament to 40 DEG C and preserving heat for 1 to 2 hours. A product prepared by the method has full appearance, looseness, high dissolubility, quick re-dissolution, high clarity and high stability.
WO2007038796A1 Formulations with improved bioavailability, comprising a steroid derivative and a polyglycolysed glyceride Compositions comprising a polyglycolysed glyceride, such as GELUCIRE, and a steroid related compound are provided.
WO2005102309A3 In vivo release of endogenous anti-microbial mediators by leukotriene b4 (ltb4) administration The invention relates to the in vivo release of endogenous anti-microbial mediators using leukotriene B4 administration. The present invention furthermore relates to the use of leukotriene B4 for the treatment and/or prophylaxis of diseases that are positively influenced by such anti-microbial mediators.
CN1850064A Preparation for relieving stress symptom The present invention relates to a preparation mainly for preventing and curing the diseases of tonicity, dysphoria, lassitude, light-headedness, hypomnesis and female premenstrual syndrome. It is characterized by that said preparation contains gamma-aminobutyric acid and theanine. Besides, in said preparation the medicinal plant, amino acid, vitamin, mineral and auxiliary material which can be used as additive in food or medicine also can be added.
CN1857211A Slow released injection containing Nolatrexed and its synergist The slow released injection containing both Nolatrexed and its synergist consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is antimetabolite Nolatrexed, Emtricitabine, etc and/or antimetabolite synergist selected from toporase inhibitor and/or tetrazine compound. The slow releasing supplementary material is selected from difatty acid-sebacic acid copolymer, polylactic acid, EVAc, and their composition. The suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for raising the effect of chemotherapeutic medicine, radiotherapeutic medicine, etc.
US20080279923 Use of Microtubule Stabilizing Compounds for the Treatment of Lesions of Cns Axons The present invention provides a use of one or more microtubule stabilizing compounds for the preparation of a pharmaceutical composition for the treatment of lesions of CNS axons wherein the pharmaceutical composition is administered locally directly into the lesion or immediately adjacent thereto, whereby the one or more compound(s) is/are selected from the group consisting of taxanes, epothilones, laulimalides, sesquiterpene lactones, sarcodictyins, diterpenoids, peloruside A, discodermolide, dicoumarol, ferulenol, NSC12983, taccalonolide A, taccalonolide E, Rhazinilam, nordihydroguaiaretic acid (NDGA), GS-164, borneol esters, Synstab A, Tubercidin and FR182877 (WS9885B). Furthermore, the invention provides a method for the treatment of lesions of CNS axons the method comprising the step of administering to a patient in the need thereof a pharmaceutical composition comprising (i) one or more microtubule stabilizing compounds selected from the group consisting of taxanes, epothilones, laulimalides, sesquiterpene lactones, sarcodictyins, diterpenoids, peloruside A, discodermolide, dicoumarol, ferulenol, NSC12983, taccalonolide A, taccalonolide E, Rhazinilam, nordihydroguaiaretic acid (NDGA), GS-164,′ borneol esters, Synstab A, Tubercidin and FR182877 (WS9885B) and, optionally, (ii) further comprising suitable formulations of carrier, stabilizers and/or excipients, wherein the pharmaceutical composition is administered locally directly into the lesion or immediately adjacent thereto.
US7488734 Anticancer agents; hormone replacement therapy; contraceptives The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
CN103172612A Dibenzo iodonium salts and anticancer application thereof The invention relates to dibenzo iodonium salts represented by the following structural formula (I), and discloses a preparation method and an application thereof. In in-vitro experiments, the iodonium salts substantially inhibit the growths of cells of human-sourced pancreatic cancer, stomach cancer, colon cancer and other malignant tumors, and provide substantially killing effects against cells of ovarian cancer, lung cancer, liver cancer, leukemia, glioma, bone marrow cancer and other malignant tumors. In animal experiments, with the salts, the growths of human pancreatic cancer and colon cancer xenografts in nude mice can be substantially inhibited. The compounds can be used in developing novel antitumor medicines. (I) is shown below.
CN101336896A New use of sodium houttutfonate injection in aspect of enhancing poultry immunity The invention discloses an application of sodium new houttuyfonate injection in enhancing immunity of poultry. Experiments can test the effect of sodium new houttuyfonate on proliferation of lymphocytes, so as to determine the in vitro stimulatory effect of sodium new houttuyfonate on the proliferation of lymphocytes and the optimal dosage. Experiments can test the anti-NDV hemagglutination inhibition antibody level in different groups of animals and the CD4<+>/CD8<+> lymphocyte ratio in peripheral blood, so as to determine the in vitro stimulatory effect of sodium new houttuyfonate on the proliferation of lymphocytes and the optimal dosage. Experiments can test the anti-NDV hemagglutination inhibition antibody level in different groups of animals, so as to determine the antagonistic action of sodium new houttuyfonate on immunosuppression in chicken caused by florfenicol and the optimal dosage. The above experimental system studies the enhancement effect of sodium new houttuyfonate on the immunity of poultry, and further enriches and perfects the immunopharmacological theory of sodium new houttuyfonate.
EP1123100B1 Improving memory by the administration of delta 5-androstene-3 beta-ol-7,17-dione and 3 beta esters thereof The memory of a healthy mammal and the memory of a mammal with age impaired memory can be improved by administering an effective amount of DELTA 5-Androstene-3 beta -ol-7,17-dione and 3 beta esters thereof.
CN101423519A Tetrandrine organic acid salt as well as preparation method and application The invention provides tetrandrine organic acid salts. White citric acid tetrandrine salt crystal is prepared through adding tetrandrine to citric acid solution to carry out salt-forming reaction, and drying the obtained tetrandrin citric acid salt solvent. The invention is proved through pharmacological test to have wider and stronger antineoplastic activity, and is proved through in-vitro cell culture system and animal test to have no obvious toxic or side effects on cell growth of a normal person and a tested animal with effective antineoplastic dosage, and have good safety, good water solubility and pH value approximate to the physiological status of human blood, thereby facilitating the improvement on bioavailability and drug action. The tetrandrine organic acid salts can be applied to preparing medicine for treating neopastic diseases. The preparation method has the advantages of simple and feasible process, high success ratio and low cost, and is applicable to scale production. The structural general formula of the tetrandrine organic acid salts is shown as the above.
US8586291 Mutations in the Bcr-Abl tyrosine kinase associated with resistance to ST1-571 The invention described herein relates to novel genes and their encoded proteins, termed Mutants Associated with Resistance to STI-571 (e.g., T315I Bcr-Abl), and to diagnostic and therapeutic methods and compositions useful in the management of various cancers that express MARS. The invention further provides methods for identifying molecules that bind to and/or modulate the functional activity of MARS.
WO2012030944A3 Quinoline and isoquinoline derivatives for use as jak modulators Provided herein are compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
EP1867330A1 Method of improving the storage stability of substance The present invention relates to a method of improving storage stability of reduced form of nicotinamide adenine dinucleotide, reduced form of nicotinamide adenine dinucleotide phosphate, or a salt thereof, or ascorbic acid, an ascorbic acid derivative, or a salt thereof, which comprises allowing the substance to coexist with an L-arginine acidic amino acid salt, a composition containing the substance and an L-arginine acidic amino acid salt, a process for producing the composition, and a method of storing the substance in the presence of an L-arginine acidic amino acid salt.
WO2013053485A1 Formulations containing quetiapine The invention relates to a quetiapine granulate consisting of quetiapine or a salt thereof, a copolymer of methacrylic acid esters, and a sugar alcohol, wherein the mass ratio between quetiapine or a salt thereof and the copolymer of methacrylic acid esters is 3:1 to 12:1, preferably 5:1 to 10:1. The invention further relates to a method for producing the granulate according to the invention, to tablets which contain said granulate, and to the use of said tablets for treating schizophrenia or anxiety. The invention further relates to a functional coating for coating the tablets according to the invention.
CN101096370A Valine entecavir and preparation method and application The invention discloses a valine Entikawei and making method and the application in the medical domain, which comprises the following steps: adopting Entikawei as raw material; esterifying; reducing; obtaining the product with good solubility and stability to improve the biological utility of agent.
CN101328159A Taxone precursor anti-cancer drugs, medicinal composition and use thereof The invention relates to a taxane precursor anticancer drug which can be reduced by an organism and has a formula (I) or a salt acceptable in pharmacology, wherein the definitions of R1-R5 are stated in the instruction. The invention also provides a medicine composition containing the compound shown in the formula (I) and an application of the compound shown in the formula (I) to the preparation of the medicine for treating proliferative diseases.
USRE38963 for treating a migraine, disorders associated with inflammation, menstrual disorders, respiratory disorders, gastrointestinal afflications, skin disorders The present invention relates to new pyazoline derivatives of formula and to physiologically acceptable salts thereof, to the method for their preparation and to their application as medicaments.
CN100999495A Compound of styryl with axa-containing heterocyclic modified and use thereof This invention relates to an azacyclo-modified styrene compounds and its applications. Its purpose is to provide an azacyclo-modified styrene compounds, and its applications in the preparation of Alzheimer's disease, Parkinson's disease and other degenerative nervous system disease or type two diabetes prevention and therapeutic drug. Studies show that the invention can inhibit aggregation of A beta, also can make the A beta aggregate depolymerizate, and will eventually hydrolysis and eliminate A beta protein, inhibited and removal of A beta toxicity, in the field of medicine has broad application prospects.
WO2006066511A1 Diazene-bridged crown ether lithium compounds and methods for their use This invention provides a method for treating an eye disease in a patient comprising: providing a photosensitive prodrug that releases upon exposure to light an active ingredient to treat the eye disease; administering the prodrug in a pharmaceutically accepted vehicle to the subject, and exposing the eye of the subject to an external light source to cause the prodrug to release the active ingredient. This invention also provides a composition for the treatment of glaucoma, comprising a compound containing a lithium ion-chelated in a crown ether- or aza-crown ether-containing chromene or diazene derivative and a pharmaceutically acceptable carrier.
CN103585128A Medicine composition containing colesevelam hydrochloride and preparation method thereof The invention relates to a medicine composition containing colesevelam hydrochloride and a preparation method thereof. A prescription of the composition comprises a main medicine of colesevelam hydrochloride and two necessary auxiliaries of silicified microcrystalline cellulose and lubricant; the preparation method avoids the complex technique in the wet granulation or the dry granulation, and overcomes the defects of weak tablet fluidity, weak content uniformity, overgreat tablet weight and low compliance of patients of the large-dosage main medicine; the medicine composition can be prepared through the preparation technology of direct powder compression. The colesevelam hydrochloride tablet prescription of the invention has the advantages of rationality, simple and stable preparation technique, better effect on the selection of the auxiliaries and the ratio selection of the main material and the auxiliaries, lower production cost and convenience in industrial application.
US20100261731 Method for Treating a Disease, Disorder or Adverse Effect Caused by an Elevated Serum Concentration of an UGT1A1 Substrate The present invention is directed to a method for inducing UGT1A1 isoform expression for treatment of a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1 substrate comprising the step of administering to a subject an effective amount of ritonavir. In particular, the present invention is directed to a method of treating unconjugated hyperbilirubinemia by UGT1A1 induction comprising the step of administering to a subject an effective amount of ritonavir.
CN103275081A Carbapenems antibiotics The invention belongs to the field of medicine technology, more specifically relates to carbapenems antibiotics, and pharmaceutically acceptable salt, hydrolyzed ester, isomer, hydrate, hydrate of ester or salt thereof shown in the general formula (I), wherein, R1, R2, R3 and ring A are defined in the specification; the invention also relates to the preparation method of compounds, and pharmaceutical composition containing the compounds, and purposes of the compounds in preparation of medicaments for infectious disease treatment and/or prevention.
US20120202843 H3K27me3 and Cancer Methods of diagnosing and monitoring cancers and precancerous lesions associated with human papillomavirus (HPV), by detecting abnormal levels of lysine (K)-specific demethylase 6A (KDM6A), KDM6B, or trimethylated Histone H3 Lys27 (H3K27me3).
WO2006062972A3 Heterocyclic compounds as inhibitors of factor viia The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
CN102670517A Method for preparing galactosyl chitosan/5-fluorouracil nanoparticle The invention provides a method for preparing galactosyl chitosan (GC)/5-fluorouracil (5-FU) nanoparticle. A GC nano material is dissolved in an organic acid to be mixed with a 5-FU sulfate solution, and a suspension mixing is performed to obtain a GC/5-FU nanoparticle. According to the prepared GC/5-FU nanoparticle, high drug loading rate and entrapment rate can be achieved, the nanoparticle is spherical, the surface is smooth, the agglomerate phenomenon is absent, a suitable particle size enables a nanoparticle carrying drugs to enter into tumor gaps but not to enter into normal tissues, and the nanoparticle can have a good targeting.
WO2008050698A2 Agent for prophylaxis or treatment of alcohol dependence or drug dependence The present invention provides an agent for the prophylaxis or treatment of substance abuse and dependence, which contains a compound of the formula (I) represented by (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide, or a pharmaceutically acceptable salt thereof as an active ingredient.
CN1891687A Inflammatory factor receptor antagonistic active compound from microbe and its use This invention relates to rivalry active compound of inflammatory factor receptors origin from microorganisms, which especially refers to the rivalry active compound or acceptable derivates of tumour necrosis factor receptor (TNFR) and interleukin-6 receptor (IL-6). The invention also relates to the method for synthesizing the medicine for the disease treatment which is caused by excessive volume of ligand of natural tumor necrosis factor receptor (TNFR) and interleukin-6 receptor (IL-6R). In addition, the invention also relates to the medicine containing the described compounds.
CN102349908A Application of dexrazoxane in preparation of drug for treating neurodegenerative diseases The invention provides application of dexrazoxane in preparation of drug for treating neurodegenerative diseases. Experiments prove that dexrazoxane can improve the behavior disorder of model rats of Parkinson's disease belonging to neurodegenerative diseases, inhibit the decrease of TH (helper T cell) nerve cells in mouse mesencephalic SNc (substantia nigra compact part) and ventral tegmental area (VTA), which is caused by MPTP/p (1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine/probenecid) modeling, improve the proliferation and activation of astrocyte and microglia, obviously inhibit the over-expression of alpha-synuclein in substantia nigra compact part and reticular part, and inhibit the reduction of survival rate of dopaminergic neuron cell strain SH-SY5Y cells, which is caused by H2O2 and MPP<+> (1-methyl-4-phenylpyridinium ion). The results show that dexrazoxane has the action of treating neurodegenerative diseases. Through the invention, dexrazoxane can be used as an active ingredient to prepare the drug for treating neurodegenerative diseases.
CN102688258A Medicine for external use for treating psoriasis, leucoderma, fungus infection and bromhidrosis The invention relates to a medicine for external use for treating skin diseases, and in particular relates to a medicine for external use for treating psoriasis, leucoderma, fungus infection and bromhidrosis, aiming at making up the defects of the existing medicine for external use for treating psoriasis, leucoderma, fungus infection and bromhidrosis; the medicine for external use comprises silver element and a pharmaceutically acceptable carrier, wherein the content of the silver element is 0.000001-0.005g/ml; and the silver element is one in nano-silver, silver salt, salt solution of silver or complexing silver, or mixture formed by mixing several in nano-silver, silver salt, salt solution of silver and complexing silver according to any proportion. By a plurality of years of clinical experience, the study for the drug properties and the observation for the treatment effect of the medicine of the inventor, the components and the ratio of the medicine are adjusted for a plurality of times, and the formulation of the medicine for external use is finally confirmed; the medicine for external use effectively reduces the medication time of a patient, thus reducing the treatment cost; and the medicine for external use is ideal is treatment effect, higher in cure rate and lower in recurrence rate, thus having important clinical significance as well as higher social value and marketable value.
US20130030038 Dermatological, Pharmaceutical Composition Suitable for Oligonucleotides The invention relates to a cosmetic and/or dermatological and/or pharmaceutical composition for the topical use and application of oligonucleotides, in particular antisense-oligonucleotides such as DNAzyme, siRNAs, asDNAs or ribozymes for use as an agent against inflammatory diseases by means of emulsions having a dispersed, internal, discontinuous aqueous phase.
US20090137530 Amine Compound and Use Thereof for Medical Purposes A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(═O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH═CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.
WO2010111934A1 Lithium derivatives of pyrroloquinoline quinone and preparation method thereof Lithium derivatives of pyrroloquinoline quinone and preparation method thereof are disclosed. In said method, lithium derivatives of pyrroloquinoline quinone are obtained by an acid-base neutralization reaction in a basic solvent with pyrroloquinoline quinine (PQQ) as a starting material. Lithium ion is brought in the molecular structure of pyrroloquinoline quinone to form said lithium derivatives of pyrroloquinoline quinone. The reaction condition of said method is mild, the product is easy to be purified, the preparation procedure is simple, and the yield is more than 80 %. Said lithium derivatives of pyrroloquinoline quinone possess GSK-3 inhibiting activity and possess the functions such as reducing the formation of age pigment in the brain of a transgenic mouse and reducing the phosphorylation of tau proteins. Said lithium derivatives of pyrroloquinoline quinone may be used in the manufacture of medicaments for preventing and treating senile dementia, senility or Parkinson's disease.
US20080255218 N-benzylamino cyclic thioureas; obesity and related disorders; (N-(3-{(4S)-1-[(1S)-2-(benzylamino)-1-methylethyl]-3-[2-(3-fluorophenyl)ethyl]-2-thioxoimidazolidin-4-yl}propyl)guanidine This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).
EP1522305A1 Combinations of sumatriptan with a cyclooxygenase II inhibitor A method of treating conditions associated with cephalic pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, sumatriptan or a pharmaceutically acceptable salt or solvate thereof and 2-(4-ethoxy-phenyl)-3-(4-methanesulfonyl-phenyl)-pyrazolo[1,5-b]pyridazine or a phamaceutically acceptable salt or solvate thereof.
CN102988396A Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor The invention provides an application of Houttuynoid D in preparation of a monoamine oxidase (MAO) inhibitor. Compared with that of the existing MAO inhibitor, the inhibitory activity and selectivity on MAO-A and MAO-B are greatly improved. The application of Houttuynoid D in preparation of the MAO inhibitor is disclosed for the first time, and because the framework type belongs to a novel framework type, the inhibitory activity on the MAO is unexpectedly high, the possibility that other compounds give enlightenment is avoided, and the Houttuynoid D has outstanding substantial characteristics and has obvious progress in treatment of MAO disorder related diseases.
US20110281837 3-substituted-6-aryl pyridines 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
WO2007025940A1 Substituted biaryls and their use as factor xa inhibitors The present invention provides compounds of the general formula in which A, B, L, R1, R2, R3a and R3b are as defined in claim 1, their tautomers, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically tolerated salts with organic or inorganic acids or bases, which exhibit valuable properties, in particular an anti-thrombotic effect and a factor Xa-inhibitory effect.
EP2117552A1 Use of condensed pyrimidine derivatives for the treatment of autoimmune and inflammatory diseases The invention relates to the use of a compound of the formula (I), or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for use in modulating an immune or inflammatory response: wherein: Z = O or S; n = 1 - 3; R3 = -CO2R8, -C(O)SR8, -C(O)NHR8, -C(S)OR8, -C(S)SR8, -C(S)NHR8, -C(NH)SR8 or -C(NH)NHR8, wherein R8 is -H or alkyl; R4 = -H, -CH2R5 or -CH2CH2R5, wherein R5 independently has one of the meanings of R3; B = -NR2-, -CH2NR2-, -CH2CH2NR2-, -CH2CHR7- or -CH2O-, wherein R2 is H or a C1-3 alkyl, alkenyl or alkynyl group, and R7 is H or a C1-3 alkyl or alkoxy group; A = wherein R1 = -NH2 or -OH, C and D are each, independently, a 5- or 6-membered, substituted or unsubstituted, aromatic or non-aromatic ring which may also contain one or more heteroatoms, and C is connected to group B in any available position.
US7229997 1-(pyridin-2-yl)-piperazine derivatives; serotonin receptor antagonists Compounds of the general formula (I): wherein R1, R2, R3 and R4 are as described in the specification. Further included are pharmaceutical compositions comprising the compounds, processes for their preparation, as well as the use of the compounds for the preparation of a medicament which particularly acts on the central nervous system, particularly for use as anti-obesity agents.
US7053116 Contacting cells with phenyl benzopyranone compound or or enantiomers, diastereomeric isomers or mixtures of any two or more thereof, or pharmaceutically acceptable salts thereof for blocking amyloid toxicity in cells In accordance with the present invention, there are provided novel methods of blocking amyloid protein toxicity in cells using polycylic compounds. Also provided are novel methods of decreasing amyloid protein production in cells and methods of inhibiting cell death. Invention methods can be used to prevent and treat a diverse class of disease conditions, known as amyloidoses, which are all related to the occurrence of amyloid protein deposits. Invention methods further provide methods of identifying compounds that can block amyloid toxicity or block the amyloid protein induced inhibition of MMT reduction.
CN103142611A Pharmacy application of composite product in treating bacterium infection The invention relates to application of medicine composite in treating respiratory system diseases. The bacterium removal rate, the clinical cure rate and the clinical recovery rate for patients of moderate and severe respiratory system diseases caused by acinetobacter baumanii of single-drug-tolerance beta-lactamase are all 100%.
US7834014 Parkinson's disease; [2-(7-amino-2-furan-2-yl-[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)-octahydro-pyrido[1,2-a]pyrazin-7-yl]-methanol; The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkinson's disease. In one embodiment, the invention features a compound of formula (I).
US7893065 mitogen activated protein kinase inhibitors; 4-(2-Fluoro-4-(methylthio)phenylamino)-N-(2-hydroxyethoxy)-1-methyl-6-oxo-1,6-dihydropyridazine-3-carboxamide; used in the treatment of hyperproliferative diseases, such as cancer and inflammation in mammals Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and W are as defined in the specification. Such compounds are MEK inhibitors and are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative and inflammatory diseases in mammals and pharmaceutical compositions containing such compounds.
US8236836 Composition comprising at least one oxazoline for inhibiting langerhans cell migration, and uses thereof The invention concerns a composition containing at least an oxazolin, optionally combined with at least a compound such as a metalloprotease inhibitor, a PKC inhibitor, an anti-inflammatory agent, a soothing agent, an immunosuppressor, an ion chelating agent, an alkanolamide, an oxazolidinone and a carbamic acid derivative. The invention also concerns the use of such a composition as medicine, in particular for preventing or treating skin pathologies of allergic and/or inflammatory and/or irritative origin or resulting from a danger signal. The invention further concerns a method for cosmetic treatment of sensitive, irritated, intolerant, allergy-prone, ageing skin and/or mucosa exhibiting skin barrier disorder, or exhibiting non-pathological immunologic imbalance, which consists in applying such composition on the skin and/or mucosa.
CN103565819A Composition for inhibiting tumor stem cells The invention provides a composition for inhibiting tumor stem cells. The composition is prepared from a curcumin extract, a piperine extract, a grifola frondosa D-fraction extract and organic selenium, wherein the piperine in the composition improves the bioavailability and antitumor activity of the curcumin, under the assistance of the antitumor effect of the grifola frondosa D-fraction and the organic selenium, the composition targets the tumor stem cells so as to kill the tumor stem cells, improve the curative effect of chemotherapeutic drugs and prevent the recurrence and metastasis of tumors. The composition can be made into tablets, capsules or oral liquid and is used for preparing antitumor drugs or healthcare food.
EP1505982A1 Trimegestone and estrogens for treating post menopausal disorders This invention relates to methods for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the sequential administration of combinations of conjugated estrogens and trimegestone.
CN101104628A 6-oxy-caffeoyl-arbutin, rock tea extract containing the same and preparation method The invention relates to a 6-O-caffeoyl-Arbutin, and an extract and a preparation method of a rock tea containing the 6-O-caffeoyl-Arbutin. The rock tea is used as the raw material, the 6-O-caffeoyl-Arbutin is extracted through the process of extraction, concentration, separation, purification, crystallization and drying in extraction solvent. Water or lower alcohol is used as the solvent in which the rock tea is heated, separated and purified in column chromatography and recrystallized, and then the 6-O-caffeoyl-Arbutin is extracted from the rock tea. The extracted 6-O-caffeoyl-Arbutin is in light yellow color powder, bitter and is easy to dissolve in the water, whose melting point is 200 DEG C. The weight content of the 6-O-caffeoyl-Arbutin in the extract is over 80 percent by the determination of high performance liquid.
US7479497 e.g. 8-hydroxy-2-[2-[3,4-dihydroxy-5-methoxyphenyl)ethenyl]]-7-quinoline carboxylic acid; HIV integrase inhibitors; AIDS, retroviral pathologies The invention relates to the use of 8-hydroxyquinoline 7-carboxylic acid derivatives in order to produce integrase-inhibiting medicaments, capable of blocking viral replication in the stages preceding integration, and if appropriate at the level of this integration stage, these medicaments being usable for the treatment of retroviral pathologies, in particular for the treatment of AIDS.
US6911442 Has no toxicological effects; adapted for oral, topical or parenteral use and may be used for the treatment of bacterial infection in mammals The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and/or N-oxide thereof: corresponding novel medicaments, pharmaceutical compositions and/or methods of
CN103159715A 17-hydrogen-9-dehydro-andrographolidume-14-sulfate, preparation method and purposes of medicine prepared by the same The invention discloses 17-hydrogen-9-dehydro-andrographolidume-14-sulfate or salt thereof, a preparation method thereof, and antipyretic, anti-inflammatory and antiviral purposes of the 17-hydrogen-9-dehydro-andrographolidume-14-sulfate or the salt thereof. The 17-hydrogen-9-dehydro-andrographolidume-14-sulfate or the salt thereof formed by the preparation method does not change chemical properties of andrographolidume, the 17-hydrogen-9-dehydro-andrographolidume-14-sulfate or the salt thereof has the advantages of being good in water-solubility, high in heat stability, small in hemoclasis, and the like, and pharmacoactive effects of andrographolidume pure natural medicine are guaranteed to the greatest extent. In addition, medicine and pharmaceutical research workers cannot know the good purposes of 17-hydrogen-9-dehydro-andrographolidume-14-sodium sulfate in advance on the premise that related experiments are not conducted.
US20120128786 Delivery System Comprising A Silicon-Containing Material A composition comprising nanoparticles of a hydrolysable silicon-contain material for use as a delivery system for a bioactive ingredient, wherein surface of the silicon-containing material is associated with a stabilizing agent which modifies the rate of hydrolysis of the silicon-contain material and/or inhibits the rate of orthosilicic acid polymerisation and a method of promoting the controlled release of orthosilicic acid on degradation of a composition comprising nanoparticles of a hydrolysable silicon-contain material, the method involving the treatment of the surface of the silicon-containing material with a stabilizing agent to modify the rate of hydrolysis of the silicon-containing material and/or inhibit the rate of orthosilicic acid polymerisation.
WO2009067699A2 Methods for providing a system of care for an oxazaphosphorine drug regimen The present invention provides methods of treating subjects with an oxazaphosphorines, methods of identifying subjects that are suitable for oxazaphosphorine treatment, and systems for ensuring the safety and efficacy of a treatment that includes oxazaphosphorine administration.
US8377913 Vitamin D receptor activators and methods of making The invention relates to compounds that are vitamin D receptor activators, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.
CN103333168A Amide compound, and preparation method and application thereof The invention discloses an amide compound, and a preparation method and application thereof. The structural formula of the amide compound is shown in a formula I or II, wherein R1 and R2 in the formula represent H, methyl, trifluoromethyl or halogen, and are the same or different; R3 represents H, hydroxymethyl, aminomethyl or C1-2 alkyl carboxylic ester; R4 represents H, methyl or isopropyl; X represents CH, N or O; and n is an integer between 0 to 3. The invention also provides a pharmaceutically acceptable salt of the amide compound shown in the formula I or II. The preparation method provided by the invention is started from simple and readily available raw materials, and an imidazole [1,2-a][1,8]-naphthyridine amide compound is obtained by reaction of 4 to 5 steps. The amide compound has high activity in the suppression of a hepatitis C virus (HCV).
US20120059006 Sigma receptor inhibitors The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
EP2459215A1 Method and kit for treating nicotine addiction Described are methods and kits related to treating nicotine addiction and increasing the likelihood of nicotine abstinence. Methods and kits for reestablishing nicotine abstinence after a relapse to nicotine use are also described. The methods and kits comprise a combination of (a) one or more of a nicotine immunogenic composition and / or an anti-nicotine antibody- composition and (b) one or more compounds selected from the group consisting of a second nicotine immunogenic composition, a second anti-nicotine antibody, a nicotine receptor agonist and a nicotine receptor antagonist.
US20140142195 Methods for the alleviation of sexual dysfunction in women This invention relates to a method for inhibition of skin atrophy, or epithelial or mucosal atrophy in women, or to a method for treatment or prevention of symptoms related to said atrophy, said method comprising administering to the woman an effective amount of the compound of formula (I) or a geometric isomer, a stereoisomer, a pharmaceutically acceptable salt, an ester thereof or a metabolite thereof.
CN103665042A Optically active 2-hydroxyltetrahydrothienopyridine derivative as well as preparation method and use thereof The invention provides an optically active 2-hydroxyltetrahydrothienopyridine derivative shown by formula I, or a pharmaceutically acceptable salt, solvate, polycrystal, enantiomer or racemization mixture thereof, wherein in the formula I, R1 is F, Cl, Br or I; m is 0 or 1; n is an integer from 1 to 6; R2 or R3 is independently hydrogen, C1-C6 alkyl or optionally substituted C1-6 alkyl; R4 or R5 is independently hydrogen, C1-C10 alkyl, C1-C10 alkenyl, C1-10 alkoxy, C1-10 aryl, halogen, acylamino, sulfmidyl, acyloxy or C(O)R', and R' is hydrogen, C1-C10 alkyl, C1-C10 alkenyl, C1-10 alkoxy, C1-10 aryl, halogen, acylamino, sulfmidyl or acyloxy. The compound has obvious platelet agglomeration resistance action, and the bioavailability of the compound is obviously higher than that of clopidogrel. The invention further provides a preparation method of the compound, a pharmaceutical composition containing the compound, and a pharmaceutical use of the compound and the pharmaceutical composition.
EP1304992B1 Topical gel delivery systems for treating skin disorders A composition is provided that has a viscosity of less than about 15,000 cP and a pH of about 3.0 to 9.0 for treating a skin disorder in a human subject. The composition consists essentially of (a) a therapeutically-effective amount of at least one compound useful for treating such disorder, (b) a pharmaceutically-acceptable, lightly cross-linked polyacrylic acid polymer compatible with the compound, (c) optionally a water miscible solvent, (d) optionally a preservative, (e) optionally an oil phase component and suitable surfactant, and (f) water. The composition is useful for treating an inflammatory skin disorder, acne, or rosacea. The low viscosity composition has an advantage of being administered more accurately when combined with a container that administers the composition as drops.
US20080108645 Dihydrotetrabenazines And Pharmaceutical Compositions Containing Them The invention provides novel isomers of dihydrotetrabenazine, individual enantiomers and mixtures thereof wherein the dihydrotetrabenazine is a 3,11 b-cis-dihydrotetrabenazine. Also provided are methods for the preparation of the novel isomers, pharmaceutical compositions containing them and their use in treating hyperkinetic movement disorders such as Huntington's disease, hemiballismus, senile chorea, tic, tardive dyskinesia and Tourette's syndrome.
US20120219596 Injectable formulation for treatment and protection of patients having an inflammatory reaction or an ischemia-reperfusion event Compounds according to formula (I) are particularly suitable for the treatment and/or prevention of a medical condition involving hypoxic, anoxic and/or inflamed mammalian tissue. Furthermore, the invention relates to the use of said compounds for preparing a medicament and to pharmaceutical preparations comprising such compounds. The invention also relates to methods of treating or protecting patients having or being prone to develop a medical condition involving hypoxic, anoxic and/or inflamed mammalian tissue, the methods comprising administration of a therapeutically effective amount of such compounds
US20120041062 Compound of salvianolic acid l, preparation method and use thereof The present invention relates to a new compound of salvianolic acid L, its preparation method, a pharmaceutical composition containing the salvianolic acid L, and its use for preparing a medicament for treating cardio-cerebrovascular diseases.
CN103301481A Target nucleic acid drug delivery system and application thereof The invention discloses a target nucleic acid drug delivery system. The target nucleic acid drug delivery system (nanometer train) disclosed by the invention maintains the recognition specificity on a target cell by an original aptamer and can deliver a loaded drug to a disease target cell in a targeting manner; a biological imaging agent delivered to the disease cell can be applied to biological diagnosis; and the drug delivered to the target disease cell can be gradually released to specifically kill the target cell. The specific killing effect reduces side effect and improves curative effect. The preparation process of the system disclosed by the invention is simple, economical and efficient, and the system is especially suitable for highly sensitive diagnosis and target administration of a disease.
US20080219998 Anticoagulant for use in treatment and prevention of thrombosis or thrombin-dependent vaso-occlusive disease; selective reduction of intravascular thromboplastin antecedent activity The present invention embodies: methods; compounds, their pharmaceutically acceptable analogs, isomer, salts, hydrates, solvates and prodrug derivatives, and pharmaceutically acceptable compositions thereof that have particular biological properties; devices; diagnostic and other assays; and the uses of such methods, compounds, devices and assays. Common throughout these embodiments is specific selective reduction of intravascular thromboplastin antecedent activity, which results in a safe antithrombotic effect. A particularly prominent application or the invention relates to diagnosis and treatment of patients which have, or are at risk of, developing thrombosis, thrombotic injury, or vaso-occlusive diseases, such as myocardial infarction, stroke, restenosis after angioplasty, thrombotic diseases, etc. Another particularly prominent feature of the present invention is its high level of hemostatic safety at optimal efficacy. Also, the present invention is compatible for use in combination with other traditional therapeutic agent such as another antithrombotic, antiplatelet, thrombolytic, or anticoagulant agents.
US20080311183 Novel Inhibitors of Pyruvate Kinase as Therapeutic Agents for Cancer The present invention relates to compounds for the inhibition of pyruvate kinase and ATP production which are capable of inhibiting cancer cells proliferation.
US20070293447 Gene Therapy for Skin Disorders Using Needleless Syringes The present invention provides highly useful clinical methods for treating skin disorders, particularly intractable skin disorders. Specifically, the methods comprise injecting/subcutaneously introducing a 10 μg to 10 mg dose of a polynucleotide, such as a DNA, oligonucleotide, RNA, siRNA, and antisense, around a lesion associated with a skin disorder, such as a wound, cutaneous ulcer, or psoriasis, using a needleless syringe that injects a pharmaceutical liquid by using gas pressure or the elastic force of an elastic member to drive a piston.
US20090035215 Radiofluorination The present invention relates to novel compounds suitable for or already radiolabeled with 18F, methods of making such compounds and use of such compounds for diagnostic imaging. Such labeled compounds are characerized by Formula II, wherein the moieties F, R1, R2, B1,2, Y1,2, Z1,2 and E have the meaning as defined in the specification and claims.
WO2013035779A1 Method of analysis of intercell interactions The purpose of this invention is to provide an analysis method which, in a system in which cells derived from different individuals coexist, comprehensively and quantitatively evaluates intercell protein interactions and identifies significant interactions and strongly interdependent signals. This method of analysis of interactions of proteins between cells derived from two or more individuals involves: a step for obtaining, and grouping by individual, the expression profiles of the genes in the micro-environment in which the cells derived from two or more individuals coexist; a step for selecting combinations of two proteins that may interact intercellularly; and a step in which, out of these protein combinations, if, in one individual of the two or more individuals, the expression level of the gene encoding one of the proteins is higher than in other individuals, and if, in an other individual other than said one individual, the expression level of the gene encoding the other of the proteins is higher than in other individuals, then the interaction resulting from said protein combination is estimated, on the basis of the expression profiles, to be a more significant interaction between said cells which are derived from the two or more individuals.
CN103483262A Stable edaravone trihydrate and pharmaceutical compositions thereof The invention belongs to the technical field of medicine, and provides stable edaravone trihydrate, edaravone trihydrate pharmaceutical compositions for injection, a method for preparing the edaravone trihydrate and a method for preparing the edaravone trihydrate pharmaceutical compositions. Crude edaravone trihydrate is stirred and dissolved in an ethyl alcohol-pure water solution, the pH value is adjusted through hydrochloric acid to range from 3 to 5, and then liquor formed by mixing ethers and ketone according to the volume ratio of 1:(1-4) is added to the solution, and stirring and crystallization are carried out; filtering, collecting, washing and vacuum drying are carried out to obtain the edaravone trihydrate which is high in yield and purity and stable in quality. The edaravone trihydrate pharmaceutical compositions, for injection, prepared according to the preparation formulation and the preparation technology are stable in quality and can be easily employed in an industrialized mode.
US7612079 2-(hydroxypiperidin-1-yl or hydroxyisoalkylamino)-6(3-nitrophenylamino, 3,4-dimethoxybenzylamino, pyrid-2-yl-methylamino, pyrid-4-yl-methylamino or indan-5-amino)-9-(isopropyl or cyclopentyl)purines; cell cyclin kinase inhibitors for treating cancer, leukemia, psoriasis and neuronal apoptosis The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof wherein R2 is 2-hydroxymethylpyrrolidin-1-yl, or NHCH(R4)CH(R3)OH, wherein R3 is hydrogen or methyl and R4 is methyl, ethyl or isopropyl; R6 is 3-nitrophenylamino, 3,4-dimethoxybenzylamino, 3-iodobenzyl-amino, pyrid-2-yl-methylamino, pyrid-4-yl-methylamino or indan-5-amino; R9 is isopropyl or cyclopentanyl. In a further aspect, the invention relates to pharmaceutical compositions comprising said compounds, and the use thereof in treating antiproliferative disorders and or viral disorders.
US7348320 lower toxicity and higher selectivity The present invention relates to platinum complexes containing bile acid derivatives having antitumor activity
EP2592935A2 Disinfectant and antiseptic formulation having reduced iodine content The invention is related to the use of the solution of elemental iodine prepared in an organosiloxane solvent as antiseptic or disinfectant agent and formulations suitable for such use.
CN103585632A Application of bile acid chelating agent or/and vitamin D in preparing drug for preventing and treating non-alcoholic fatty liver disease The invention belongs to the technical field of pharmaceutical preparation application, in particular to an application of a bile acid chelating agent or/and vitamin D in preparing a drug for preventing and treating a non-alcoholic fatty liver disease. The bile acid chelating agent is polyamine cation exchange resin and comprises cholestyramine, colestipol and the like, and the vitamin D is selected from vitamin D2, vitamin D3, bioactive vitamin D3 and a derivative of the bioactive vitamin D3. The chelating agent and the vitamin D can be medicated either independently or together. The chelating agent and the vitamin D are combined with intestinal bile acid to reduce fat emulsification, absorption of lipid from diets, and deposition of the lipid in a liver. After the chelating agent and the vitamin D are combined with the intestinal bile acid, liver bile acid synthesis is increased, so that endogenous fatty acid synthesis is inhibited. In addition, the active vitamin D and the derivative thereof also can inhibit inflammation, promotes intestinal reabsorption of the bile acid, inhibits the endogenous fatty acid synthesis, and therefore relieves the non-alcoholic fatty liver disease.
CN1813756A Ganciclouir dispersible tablet and its preparing method The present invention relates to a ganciclovir dispersing tablet and its preparation method. The described ganciclovir dispersing tablet contains 40-80% of ganciclovir, optimally, contains 50-65% of ganciclovir, the rest is auxiliary material which can be excipient, disintegrant, surfactant, adhesive, correctives and lubricant.
CN102657656A Composition and methods for modulating a kinase cascade The invention relates to ccompositions comprising N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide (KX2-391), and methods for modulating one or more components of a kinase cascade.
WO2013184621A1 Combination of a 17 -alpha -hydroxylase (c17, 20 - lyase) inhibitor and a specific pi-3k inhibitor for treating a tumor disease The present invention relates to a combination which comprises (a) a phosphatidylinositol 3-kinase inhibitor selected from the group consisting of a compound of formula (I) or a compound of formula (II), or pharmaceutically acceptable salt thereof, (b) a 17α-Hydroxylase/ C17,20-lyase inhibitor (CYP17 inhibitor), specifically abiraterone acetate and 1-(2-Chloro-pyridin-4-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one or pharmaceutically acceptable salt thereof, for simultaneous, separate or sequential use for the treatment of a tumor disease; a pharmaceutical composition comprising such combination; use of such combination for the treatment of a tumor disease; a commercial package or product comprising such combination; and to a method of treating a patient having a tumor disease comprising administration of said combination to a patient in need thereof.
US7015240 Treatment of macular edema The invention relates to the use of photodynamic therapy (PDT) to treat macular edemas, including DME, CRVO and BRVO. It provides an alternative to photocoagulation and the disadvantages associated therewith.
WO2013041502A1 N-[4-(1h-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
CN102127074A 6-sulfamyl substituted-beta-carboline-1-ketone cell cycle protein dependent kinase 2 inhibitor and application thereof The invention relates to the field of pharmaceutical chemistry, in particular to a 6-sulfamyl substituted-beta-carboline-1-ketone alkaloids and a preparation method thereof, a medicinal composition containing the compounds, the medical application of the compounds, and especially the usage of cell cycle protein dependent kinase 2 inhibitor.
US20120171156 Methods and compounds for reducing allergic reactions to hair dyes Conventional commercial hair dyes form potent allergens and may also have irritant properties. If they were not already well established in the market and the side effects tolerated by consumers they would likely be deemed unsafe for use. The invention relates to compounds, compositions, formulations and methods for reducing, avoiding or eliminating allergic contact dermatitis reactions to conventional commercial hair dyes.
WO2011113030A2 Human cancer micro-rna expression profiles predictive of chemo-response Disclosed are identified and successfully targeted microRNAs (miRNAs) associated with human cancer cell line response to a range of anti-cancer agents. The strategy of integrating in vitro miRNA expression and drug sensitivity data not only aid in the characterization of determinants of cytotoxic response, but also in the identification of novel therapeutic targets.
EP2766352A1 Indazole compounds as kinase inhibitors and method of treating cancer with same The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells.
US20070066593 Use of carbamazepine derivatives for the treatment of agitation in dementia patients The present invention relates to the use of a compound of formula (I) wherein (a) R1 and R2 together form an oxy group or (b) R1 is hydrogen and R2 is hydroxy or acetoxy, or a pharmaceutically acceptable salt thereof, for the manufacture of a pharmaceutical composition for the treatment of agitation, in particular behavioral agitation, especially in dementia patients; a method for the treatment of agitation; pharmaceutical compositions comprising a compound of formula I; a combination comprising (a) a compound of formula I and (b) at least one compound selected from the group consisting of nootropic plant extracts, calcium antagonists, cholinesterase inhibitors, dihydroergotoxin, nicergoline, piracetame, purine derivates, pyritinol, vincamine and vinpocetine; and a commercial package including such combination.
US20100015205 Biocompatible amino acid anhydride polymers Biocompatible amino acid anhydride polymers for use in tissue engineering, and methods for their preparation and use.
CN101485636B Risperidone orally disintegrating tablets and preparation method thereof The invention relates to a risperidone orally disintegrating tablet for treating mental diseases and a method for preparing the same, and belongs to the technical field of medicines. The risperidone orally disintegrating tablet comprises the following components in percentage by weight: 0.25 to 4 percent of risperidone, 85 to 91 percent of spray drying mannitol, 1 to 4 percent of cross-linking sodium carboxymethyl cellulose, 2 to 6 percent of carboxymethyl starch sodium, 0.5 to 2 percent of miropowder silica gel, 0.5 to 2 percent of magnesium stearate, 0 to 2 percent of sweet agent, and 0 to 2 percent of flavoring agent. The raw materials are evenly mixed, and the fine powder is directly tableted. The risperidone orally disintegrating tablet has enough hardness, and can meet requirements on production, packaging, storage and transportation; and simultaneously, the risperidone orally disintegrating tablet also has good taste and short disintegration time.
DE102008004100A1 New metallocene compounds are estrogen receptor modulators useful e.g. to treat preferably cancer, manic disorder, gynecomastia and/or female infertility, and to prevent mamma carcinoma Metallocene compounds (I), are new. Metallocene compounds of formula (I), are new. M : Fe, Ru, Os, Co, Rh or Ir; R1a-R1d, R2a-R2d : H, alkyl, halo, OH, NH 2, SH, CH 2(CH2) 0-20OH, CH 2(CH2) 0-20NH 2, CH 2(CH 2) 0-20SH, C(O)OH, P(alkyl) rH 3-r, P(aryl)SH 3-s, aromatic, olefin and/or aliphatic carbo- or heterocycle; X, Y1, Z : (-C(R3)(R4)-), (-C(R5)(R6)-) or (-C(=C(R7)(R8))-); either R3-R6 : H, halo, pseudo halo, OH, NH 2, SH, alkyl, alkoxy, alkyl amino, dialkyl amino, alkylthio, aryl, aryl alkyl, aryloxy, arylalkyloxy, heteroaryl or heteroarylalkyl; or R3R4, R5R6 : O, imino or an alkyl substituted imino; R7, R8 : cycloalkyl, cycloalkenyl, aryl, arylalkyl, aryloxy, arylalkyloxy, heteroaryl or heteroarylalkyl (all optionally substituted); and n, m, o : 0-3. Where: n, m and o are not simultaneously 0; and at least one of the groups of X, Y1 or Z is (-C(=C(R7)(R8))-). N.B: r and s are not defined. An independent claim is included for the preparation of (I). [Image] - ACTIVITY : Cytostatic; Antimanic; Endocrine-Gen.; Antiinfertility. - MECHANISM OF ACTION : Estrogen receptor modulator.
CN101029064A Bean-curd pectin analogues, and its use in preparation of medicine for preventing senile dementia A helicidum analog with high selective suppression to acetylcholinesterase and its application in preparing the medicines for preventing and treating senile dementia are disclosed.
WO2008136059A1 Composition for improving vascular endothelial function It is intended to develop a safe composition capable of improving/ promoting the vascular endothelial function or preventing a decrease in the vascular endothelial function. The invention relates to a food or a pharmaceutical composition for improving/promoting the vascular endothelial function or preventing a decrease in the vascular endothelial function by oral intake, which contains at least one member selected from acetic acid, an acetate ion and an acetate as an active ingredient.
WO2009010480A1 1-{2-[(diphenyl)amino]-ethyl}-piperidine-4-carboxylic acid benzylamide derivatives and related compounds as ccr5 agonists for the treatment of immune and inflammatory diseases The present invention relates to pharmaceutically active piperidine derivatives and their use as agonists of CC chemokine receptor activity, more specifically of CCR5 activity. Chemokines are chemotactic cytokines which play an important role in immune and inflammatory responses.
US6881742 Benzyl amidoxime derivatives, intermediate products and method for their production and use as fungicides Novel benzamidoxime derivatives, processes and intermediates for their preparation and their use as fungicides are described. In the context of the present invention, benzamidoxime derivatives are compounds of the formula I where: A is an aryl or hetaryl radical; Y is a straight-chain or branched C1-C4-alkylene group, where one carbon can be replaced by oxygen, nitrogen or sulfur or by a cyclopropyl group; Rn 1 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy; R2 is unsubstituted or substituted phenyl-C1-C6-alkyl, thienyl-C1-C4-alkyl, or pyrazolyl-C1-C4-alkyl, Rp 3 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy, C1-C6-alkylcarbonyl; n is 0-5; p is, depending on the number of free valencies, 0-4.
CN101278930A New purpose of brevifolin A new application of brevifolin relates to the new application in medicine of the brevifolin made from pomegranate leaf, in particular to medicinal application of the brevifolin for preventing preadipocyte in body from transforming to fat cell and treating disease caused by transformation. Experiments and studies show that the brevifolin has the effects of inhibiting intracellular TG from accumulating when the preadipocyte transforms to the fat cell, the activity of intracellular 3-phosphate dehydrogenase from increasing and in the late stage of differentiation and the activity of LPG from increasing in the accumulation of the intracellular TG in the fat cell. Therefore, the brevifolin can be used for preventing and treating obesity. When treating the obesity, the brevifolin is taken as active component. Furthermore, the brevifolin can be used independently or the brevifolin and other medicine are made into medicine with different forms for clinical use.
US20090062345 Amide derivatives as trpv1 antagonists The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, and R3, are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
WO2013010881A1 NEW CRTh2 ANTAGONISTS The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
US20130071337 Interomone Compositions and Their Use to Modify Behavior in Different Vertebrate Species A composition comprising an interomone is described for the modification of undesirable or harmful stress-related behaviors or other behaviors or physiology in a variety of vertebrate species, as well as methods of using the compositions in vertebrates from a species different than the species in which the interomone is a naturally occurring pheromone.
WO2014090259A1 Product comprising red clover extract and methods for producing the same The invention relates to a composition comprising isoflavones from red clover. The red clover extract has been fermented to obtain a composition comprising aglycone isoflavones. The fermentation is preferably performed by a lactic acid bacteria or fermented dandelion extract.
WO2014009936A1 Compositions for the treatment of neuropathic pain The present invention relates to the field of compositions for the treatment of neuropathic pain. More specifically, the present invention relates to compositions comprising compounds obtained from plant extracts for the treatment of neuropathic pain caused by chemotherapeutic drugs.
CN101559061B Pharmaceutical composition and injection for treating unknown high fever of pigs and preparation method thereof The invention discloses a pharmaceutical composition for treating the unknown high fever of pigs, which comprises the following components by the weight percent: 33-60 of florfenicol, 33-60 of sulfamonomethoxine, 6-26 of diclofenac potassium and 0.3-0.6 of interferon inducer. The invention also discloses an injection for treating the unknown high fever of the pigs and a preparation method thereof.After the composition enters an organism, the cooperative action of effective constituents in the composition relieves and treats different symptoms and complications caused by highly pathogenic blue-ear diseases, and the pharmaceutical composition has high cure rate and obvious curative effect so as to realize the aim of treating both the principal and the secondary aspect of the disease.
US20100240648 Hexahydro-pyrrolo-isoquinoline compounds Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
US20090306099 Monitoring human response to antiviral agents; obtain tissue sample, extract nucleotide sequences, detect tumor necrosis factor genotype, presence of genotype indicates sensitivity to viricide; treating a male Caucasian human in need of treatment with abacavir Methods of assessing the risk of clinical signs of hypersensitivity reaction to nucleoside antiviral compounds, including abacavir, are described. The methods include genotyping subjects for polymorphisms in the TNFα gene, the class 1 HLA genes, or a combination of both the TNFα and HLA genes.
CN103408540A 2-imidazole ring-substituted thiophene PLK1 (Polo-like kinase 1) inhibitors and applications thereof The invention relates to the field of medicinal chemistry, and in particular relates to 2-imidazole ring-substituted thiophene PLK1 (Polo-like kinase 1) inhibitors, a preparation method for the inhibitors, a medicinal composition containing the compounds, and medical applications for the compounds, and in particular an application for the compounds as Polo-like kinase 1 (PLK1) inhibitors.
WO2006045963A2 Composition of cosmetic or pharmacological application for stimulation of synthesis of collagen The invention relates to a composition of cosmetic or pharmacological application for stimulation of synthesis of collagen, in particular, for stimulation of restructuring of the skin. According to the invention, the composition comprises ethanol, ethyl acetate, eucalyptol, dipropylene glycol, linalol, linalyl acetate, itaconic anhydride or methyl succinate, terpinen-4-ol, a-terpinol, camphor, bornyl acetate, geranyl formate, geraniol or geranyl acetate, coumarin and diethyl phthalate. Said composition only contains natural or very low cost compounds.
CN102335121A Preparation and application of pH sensitive in situ gel for vagina Relating to the technical field of medicines, the invention provides a new dosage form of Clindamycin phosphate, i.e. preparation and application of temperature sensitive and pH sensitive Clindamycin phosphate in situ gel. The gel is characterized by preparation and application of the gel that is a solution under a nonphysiological state and is gel through phase transition under a physiological state. The temperature sensitive and pH sensitive Clindamycin phosphate gel is finally prepared by Poloxamer 407 (F127 for short) and Poloxamer 188 (F68 for short) in a proper ratio. The pH sensitive in situ gel is prepared by Carbopol 980 and Poloxamer F127 in a proper ratio. The gel has viscosity of less than 1100mpa.s under a nonphysiological condition and viscosity of greater than 2500mpa.s under a physiological condition with pH greater than 4.5. The gel prolongs the detention time of Clindamycin phosphate in the vagina and improves the bioavailability and curative effects, thus boasting good application prospects.
CA2347474C Bicyclic nitrogen heterocycles Amino-substituted dihydropyrimido [4,5-d]pyrimidinones of formula (I) in which R1 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl, R2 represents lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl; and R3 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl, lower cycloalkenyl or lower cycloalkyl-lower alkyl, and pharmaceutically acceptable salts thereof are protein kinase inhibitors. They can be used in the treatment or prophylaxis of inflammatory, immunological, oncological, bronchopulmonary, dermatological and cardiovascular disorders, in the treatment of asthma, central nervous system disorders or diabetic complications or for the prevention of graft rejection following transplant surgery.
CN101596155A Teniposide solid lipid nanoparticle and preparation method thereof The invention discloses a teniposide solid lipid nanoparticle and a preparation method thereof in industrial application. The teniposide solid lipid nanoparticle comprises an effective treatment dose of teniposide, a lipid material and an emulsifier, has smaller grain diameter, high entrapment rate and good stability, improves the solubility and the stability of the teniposide, reduces the toxicity of the teniposide, prolongs the cycle time of medicaments in blood and improves the therapeutic index of the medicaments, thereby having the characteristics of low toxicity and irritability and high efficiency in clinical application.
WO2007008156A1 A pharmaceutical composition comprising a substituted phenylpropionic acid as a free acid and as tert-butyl amine salt thereof A pharmaceutical composition comprising a compound of formula I wherein n is 1 or 2, R1 represents hydrogen, chloro, trifluoromethyl or trifluoromethoxy, R2 represents hydrogen or fluoro and R3 represents a C2-6 alkyl group, wherein the compound of formula (I) is present in the composition as a free acid and as a tert-butyl amine salt thereof.
CN102579483A Emulsion liniment for curing mild burn and preparation method thereof The invention discloses an emulsion liniment for curing mild burn and a preparation method thereof, and belongs to the medicine for curing burn. The emulsion liniment is characterized in that the raw material components in the following weight proportions are comprised: a, 2-8 parts of calcium hydroxide saturated solution; and b, 8-2 parts of animal and vegetable oils. The invention provides an emulsion liniment for curing mild burn with advantages of improving the penetrability and stimulus of the medicine to skin and mucous membranes, eliminating the suffering of the patient during curing, being absorbed quickly, and is minimal in toxic and side effects, fast in efficacy, high in curing rate, simple in formula and low in price. The invention also provides a preparation method for preparing the emulsion liniment for curing mild burn with advantages of simple process and low production cost. The emulsion liniment for curing mild burn is a water/oil emulsion, improves the penetrability and stimulus of the medicine to skin and mucous membranes, can rapidly exert efficacy due to small, fine and disperse drops so that the medicine can be rapidly absorbed, has a quick effect, and has a 100 percent effective rate in 100 clinical treatment cases.
WO2013103250A1 Composition comprising tauroursodeoxycholic acid Provided are: a pharmaceutical composition for preventing or treating periodontal disease, said composition comprising tauroursodeoxycholic acid as an active ingredient; and a composition for improving oral hygiene.
CN102050847A Extraction and separation method of tannic acid used for curing spontaneous perspiration and night sweat, tannic acid preparation and preparation method of tannic acid preparation The invention relates to an extraction and separation method of tannic acid in the effective-part of gallnut, a tannic acid preparation and a preparation method of the tannic acid preparation. The extraction and separation method comprises the following steps: 1) cleaning and selecting medicinal material gallnut, breaking open, removing impurities; 2) grinding medicinal material gallnut, sieving with a 80 mesh sieve; 3) taking a defined amount of the grinded gallnut, adding five times of 45-55 DEG C warm water by volume to soak for 2 hours, stirring at 1000-1200rpm for 1 hour, then adding three times of water by volume to stir and extract for 1 hour, cooling the extract to 3-8 DEG C, sieving with a 200 mesh sieve; and 4) adding the filtrate in an activated carbon dry thin-film column, wherein the amount of the loaded sample is determined according to the result of thin layer chromatography; then determining the position of tannic acid in the column according to the result of thin layer chromatography, cutting the positioned tannic acid section, eluting with water, concentrating under reduced pressure and drying. The invention provides the extraction and separation method of tannic acid which has definite treatment effect and no toxic and side effect, is used for treating spontaneous perspiration and night sweat and takes effect fast and the preparation method of the tannic acid preparation.
US20120237605 Multifunctional Metal Nanoparticles Having A Polydopamine-Based Surface and Methods of Making and Using the Same The present invention provides nanoparticles including a metallic core having a length along each axis of from 1 to 100 nanometers and a coating disposed on at least part of the surface of the metallic core, wherein the coating comprises polydopamine, along with methods for making and using such nanoparticles. The metallic core may be gold, silver or iron oxide and the polydopamine coating may have other substances bound to it, such as silver, targeting ligands or antibodies, or other therapeutic or imaging contrast agents. The disclosed nanoparticles can be targeted to cells for treating cancer or bacterial infections, and for use in diagnostic imaging.
EP1420799B1 Use of atazanavir in hiv therapy A method for reducing elevated plasma LDL and/or triglyceride levels in an HIV-infected patient is disclosed. In this method, atazanavir (BMS-232632) can be used to treat HIV infection in patients exhibiting elevated plasma LDL-cholesterol and/or triglyceride levels, can be substituted for an offending HIV protease inhibitor used in such therapy, or can be used in combination with an HIV protease inhibitor metabolized by cytochrome P450 monooxygenase.
US20090030041 N-substituted N-(4-piperidinyl) Amide Derivative An N-substituted N-(4-piperininyl)amide derivative represented by the following formula (I): (wherein R1 represents C1-6 alkyl, furyl, etc.; R2 represents amino, acetylamino, ureido, etc.; R3 represents hydrogen, C2-8 alkoxycarbonyl, etc.; R4 represents optionally substituted phenyl, etc.; R5 represents hydroxyl, benzyloxy, etc.; R6 represents hydrogen or methyl; and m is 1 or 2) or a salt of the derivative, and an analgesic containing the derivative or salt.
US20100130412 Compositions to prevent and treat type-1 diabetes The present invention is based on the discovery that Humanin and humanin analogues protect pancreatic beta cells in vitro and in vivo from apoptosis. Accordingly, humanin and its analogues are useful for preventing and treating diabetes and promoting beta cell survival in a number of applications.
CN102526282A External-use health care product for lowering intraocular pressure of diabetes mellitus eye disease patient The invention relates to an external-use health care product for lowering the intraocular pressure of a diabetes mellitus eye disease patient, which is characterized in that the external-use health care product comprises 2-5mg of lycium barbarum polysaccharide, 3-7mg of rhizoma alismatis polysaccharide, 4-7mg of saffron total saponins, 4-7mg of total saponins of panax ginseng, 15-45mg of jasmine total saponins, 3-7mg of mannitol, 15-25mg of tyloxapol, 15-25mg of edetate disodium, 15-25mg of potassium chloride, 25-25mg of azone, 2-5ml of hydrochloric acid or 1-3mg of potassium hydroxide (for regulating the pH value) and 1000-3000mg of pure water. The external-use health care product has the efficacy on clearing liver, improving vision, soothing the liver, purging intense heat, carrying out miosis, relieving pain and lowering the intraocular pressure.
WO2013137628A1 Novel diacylglycerol acyltransferase-2 inhibiting material, and use thereof The present invention relates to a novel diacylglycerol acyltransferase-2 (DGAT2) inhibiting material, and to the use thereof. The DGAT2 inhibiting material of the present invention, which is expressed by the following formula 1, is a first material having the effect of selectively inhibiting DGAT2 and exhibiting almost no cytotoxicity, and is therefore useful as a composition for preventing, alleviating, or treating metabolic diseases, such as obesity, diabetes, fatty liver, hyperglycemia, and cardiovascular disorders. In addition, the DGAT2 inhibiting material of the present invention can be used as a composition for functional health foods.
WO2010018268A1 Novel (rs)-7- or 9-(1,2,3,5-tetrahydro-4,1-benzoxazepin-3-il)-7h or 9h-purines having antitumour activity The invention relates to compounds intended for use in the treatment of human and animal tumours. Experimental results obtained on breast tumour and non-tumour cells lines suggest that the selected compounds have a specific selective antitumour activity, rendering same excellent candidates for future use in the treatment of different types of cancers.
US7517998 Benzothiazole or benzothiazine derivative of dipyrido(2,3;b:2',3'-e) diazepin-6-one; viricide against human t-cell leukemia/lymphoma virus Compounds of formula (I): wherein Ar, X, R1, R2, R3 and R4 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against wild type and single or double mutant strains of HIV.
US20100303921 Pharmaceutical Compositions Comprising Cereal Beta (1-3) Beta (1-4) Glucan The present invention relates to pharmaceutical compositions comprising a β (1-3) β (1-4) glucan and a pharmaceutically active agent or a botanical extract. A method to extract and purify cereal β-glucan is also described. The high purity of the cereal β-glucan obtained according to the present invention allows for the preparation of clear, colourless viscous liquid preparations. These liquid preparations are stable to gelling effects when kept at ambient temperatures and low ash concentrations, and can be used to prepare the pharmaceutical compositions of the present invention.
CN101322713A Applications of gastrodine in preparing cysteine proteinase-3 active inhibitor The invention discloses the application of gastrodine to the preparation of caspase-3 active inhibitor and belongs to the field of pharmacy. The gastrodine is applied to the preparation of caspase-3 active inhibitor, the caspase-3 active inhibitor can be used for treating diseases including neurodegenerative diseases, cardiovascular and cerebrovascular diseases, osteoarthritis, rheumatoid arthritis, and the like, specifically such as Parkinson disease, Alzheimer disease, amyotrophic lateral sclerosis, Huntington disease, traumatic brain injury, spinal cord injury, severe hepatitis, liver dysfunction, osteoarthritis, rheumatoid arthritis, acquired immunodeficiency syndrome, myocardial infarction, cerebral ischemia and the like. The application of gastrodine has the advantage of blocking the specific protease needed by apoptosis without any adverse reaction which is caused by the application of the majority of broad spectrum drugs.
WO2014101366A1 Methods for inhibition of shc-1/p66 to combat aging-related diseases The present invention relates to methods of treating one or more symptoms of a SHC-1/p66-related disease, inhibiting ROS generation or for the manufacture of a medicament in the above-mentioned treatment.
US7960407 Crystal forms of an imidazole derivative The invention relates to the essentially pure Λ/-[({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}amino)carbonyl]-4-methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containing and to the uses of, such crystal forms.
WO2009120881A1 Methods for improving lid margin and tear film function and treatment of lid margin desease using tetracycline family antibiotics The present invention provides a mucoadhesive broad spectrum antibiotic with anti-inflammatory characteristics with strong tissue penetration for improving lid margin function and the treatment of diseases associated therewith. The present invention further provides compositions and methods for treating and/or preventing the signs and/or symptoms of blepharitis and dry eye disease.
CN103120683A Application of Aphanamixoid A in prevention and treatment of hepatic injury The invention discloses application of Aphanamixoid A in prevention and treatment of hepatic injury. The inventor performs pharmacological research on the Aphanamixoid A and then discovers that the Aphanamixoid A has protective effect on D-galactosamine (D-galactosamine, D-GalN) induced mice acute hepatic injury and has protective effect on CCl4 induced mice acute hepatic injury. Thus, the Aphanamixoid A can be used for preparing a medicine for preventing and treating hepatic injury or hepatitis.
CN103340988A External ointment for treating bedsore and preparation method thereof The invention relates to an external ointment for treating bedsore and a preparation method thereof. The external ointment is composed of total 16 medicinal materials as follows: calcined gypsum, flat-stemmed tetrastigma leaf, hedysarum polybotrys, vitis flexuosa leaves, potentilla freyniana bornm, coriaceous knotweed rhizome, concha meretricis sea cyclinae, sedum lineare, puffball, water caltrap shell, bark of Chinese redbud, basil root, Chinese incarvilla herb, huperzia serrata, calamine and borneol. The external ointment provided by the invention has the effects of promoting blood circulation to remove blood stasis, promoting tissue regeneration and relieving pain, converging wound and moisturizing skin, and is capable of improving the blood circulation of the pressed tissue of a bedridden patient, moisturizing skin, and promoting growth of new granulation tissue; the external ointment is good in effects of converging sores and promoting tissue regeneration, and thus capable of promoting quick healing of the bedsore wounds. Besides, the external ointment provided by the invention is obvious in treatment effect, low in cost, quick in taking effect and accurate in curative effect; the healed skin is as smooth as before, and has pores regrown without scars.
CN1931223A Recipe of body resistance strengthening Sisheng glossy ganoderma prepn The present invention relates to medicine and health product, and is especially one kind of medicine and health product with glossy ganoderma, tea polyphenol, and the effective matter of Brazil mushroom or astragalus root as the main materials. The medicine and health product has the functions of regulating in vivo circulation and body's immunity, strengthening physique, eliminating toxicant, protecting liver, resisting tumor, etc. and may be prepared into different forms, including capsule, tablet, pill, granule and oral liquid via adding different additives.
WO2010086736A3 Use of the combination of resveratrol with cysteine and derivatives thereof The present invention relates to a novel use of nutritional/pharmaceutical compositions comprising as active ingredients resveratrol and cysteine and derivatives thereof. More specifically, the invention relates to the use of such nutritional/pharmaceutical compositions for treating and/or preventing a hyaluronidase-related disorder such as skin senescence or joint arthritis, in particular in postmenopausal women.
WO2013010839A1 Novel and selective ccr2 antagonists The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain. Claimed are compounds of formula (I), wherein G and E are independently selected from among C-H or N; wherein A is a group selected from among wherein R6 is a group of the structure -L1-R13, wherein L1 is selected from among -NH-, and -N(C1-C4-alkyl)-, and wherein R13 is selected from among -C5-C6-heterocyclyl comprising 1 or 2 hetero atoms selected from among N, and 0, and wherein R13 is optionally substituted; The other variables are as defined in the claims
WO2007014327A3 Small compounds that correct protein misfolding and uses thereof The invention features compositions and methods comprising at least one compound selected from a proteasomal inhibitor, an autophagy inhibitor, a lysosomal inhibitor, an inhibitor of protein transport from the ER to the Golgi, an Hsp90 chaperone inhibitor, a heat shock response activator, a glycosidase inhibitor or histone deacetylase inhibitor that are useful for treating or preventing a protein conformation disease in a subject by correcting misfolded proteins in vivo. The compositions and methods can further comprise an 11-cis-retinal or 9-cis-retinal compound. Examples of protein conformation disorders and/or diseases may include retinitis pigmentosa, age-related macular degeneration, glaucoma, corneal dystrophies, retinoschises, Stargardt's disease, autosomal dominant druzen, Best's macular dystrophy, αl -antitrypsin deficiency, cystic fibrosis, Huntington's disease, Parkinson's disease, Alzheimer's disease, nephrogenic diabetes insipidus, cancer and/or Jacob-Creutzfeld disease.
WO2012116290A3 Neuroactive 17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same The present disclosure is generally directed to neuroactive 17(20)-Z-vinylcyano-substituted compound of Formula (I) and (II), as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
CN103356609A Compound intravenous anesthetic The invention discloses a compound intravenous anesthetic which comprises propofol and etomidate according to a mass ratio of (2.5-5.5):1. The compound intravenous anesthetic disclosed by the invention is high-efficiency, safe, high in controllability, slight in adverse reaction and convenient in clinical application.
CN103230431A Medicine for treating stomach disease and application The invention relates to the field of medicine, and in particular relates to a medicine for treating stomach disease and an application. The medicine for treating stomach disease comprises the following components in parts by mass: 310-620 parts of furazolidone, 202-520 parts of chloramphenicol, 105-210 parts of propantheline bromide, 2,000-3,000 parts of licorice powder and 2.01-3.95 parts of vitamin B6. The medicine is used for treating acute gastritis, chronic superficial gastritis, chronic atrophic gastritis, gastric ulcer, bile reflux gastritis or duodenal ulcer. According to the medicine for treating stomach disease and application provided by the embodiment of the invention, multiple components are combined to realize sterilization and suppression effects so as to protect and maintain the stomach; and the raw materials are rich, the price is low, and the treatment cost is lower. In a process of treating stomach disease, the medicine has the advantages of high cure rate, short cure time, perfect effect, simplicity and convenience in preparation, simple preparation flow of technological medicines and obvious curative effect, is safe to take, and avoids adverse reaction.
WO2009025571A1 Sublingual or buccal pharmaceutical compositions comprising succinic acid for treating alzheimer's disease The present invention relates to sublingual or buccal pharmaceutical compositions for preventing and/or treating Alzheimer's disease comprising a therapeutically effective amount of succinic acid or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. Further, the present invention relates to methods for preventing and/or treating Alzheimer's disease with using compositions of the present invention.
CN101057826A Oryzanol injection with ethyl oleate as solvent and its preparation method The invention relates to an oryzanol injection which takes aethylis oleas as solvent and the preparation method. The oryzanol injection taking plant oil as solvent is characterized in that it is easy to produce deposition during storage and the quality is uncontrollable. The invention means to solve the problems. The preparation method comprises following steps: adding aethylis oleas into 10 -100g oryzanol, dissolving and fixing the volume to be 1000 ml, filtering said solution with micro-porous membrane to remove bacteria, checking and packing in the medicine bottle, sealing and getting injection. The invention can be used for oryzanol injection production and usage, and is characterized by no deposition and easy absorption.
CN102835240A Cultivation method of selenium-enriched Codonopsis lanceolata, as well as extraction method and application of selenium-containing polysaccharide of selenium-enriched Codonopsis lanceolata The invention discloses a cultivation method of selenium-enriched Codonopsis lanceolata, as well as an extraction method and an application of selenium-containing polysaccharide of the selenium-enriched Codonopsis lanceolata, wherein the selenium content in the root of Codonopsis lanceolata after selenium-enriching cultivation is improved by 18.9 times by comparison; the yield of the Codonopsis lanceolata is improved notably; the selenium-containing polysaccharide of the Codonopsis lanceolata is extracted by hot water ultrasonic extraction and microwave extraction method, therefore, the extraction time is shortened notably and the extraction ratio of the selenium-containing polysaccharide is increased; instant particles and buccal tablets prepared from the selenium-containing polysaccharide are convenient to carry and take, and have notable effects such as resisting tumor and improving immunity.
WO2008071968A1 Cucurbitacin b and uses thereof The present invention relates to uses of cucurbitacins and compositions comprising cucurbitacin B. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof cucurbitacin B. The invention also encompass methods of developing a therapeutic that comprises a cucurbitacin using the signaling molecules in the Ras-Raf-Mek-Elk-STAT3 pathway.
CN1931113A Intrauterine device of composite material The intrauterine device (IUD) of composite material consists of one vertical arm and two arc arms distributed symmetrically about the top of the vertical arm, and has also two spheres in the external ends of two arc arms and one semi-sphere in the bottom of the vertical arm and with anal filament hole in the center. It has the shape between T and Gamma, accords with the morphologic and dynamic requirements of women's uterine. Compared with available IUD, the present invention has simple setting operation without need of dilatation, no damage on endocervix and less pain, bleeding and other side effects.
CN101530618B Pharmaceutical composition for the treatment of chronic obstructive pulmonary disease and bronchial asthma The invention discloses a pharmaceutical composition for the treatment of chronic obstructive pulmonary disease (COPD) and bronchial asthma, which is composed of a glucocorticoid, a bronchodilator and a pharmaceutically acceptable auxiliary material or carrier; the composition is a preparation for oral use. The glucocorticoid in the inventive pharmaceutical composition is selected from prednisone, prednisolone, methylprednisolone, betamethasone, decamethasone or hydrocortisone; the bronchodilator is selected from formoterol, clenbuterol, procaterol or theophylline. The inventive composition has better therapeutic effect on the COPD and the bronchial asthma than independent administration of two ingredients, and has synergistic effect. The composition has easily-available raw materials, inexpensive price and increased medicine taking compliance as well as plays a significant role in preventing and treating the COPD and the bronchial asthma of patients in vast rural areas and patients in low-income class of the city in China.
US7034048 Gastrin and cholecystokinin receptor ligands (III) Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R5)—(R5 being selected from H, Me, Et, Pr, Bn, OH and —CH2COOR6, wherein R6 represents H, Me, Et, Pr or Bn), ═CH—, —O— or —S—; n is from 1 to 4; A is an optionally substituted 5- or 6-membered carbocyclic ring wherein (a) 1 or 2 C atoms may optionally be replaced by N, O and/or S atoms, (b) A is fused with the aromatic group in formula (I) to form a fused bicycle, and (c) the ring containing X and Y is linked to a C atom of A; R1 is H or C1 to C15 hydrocarbyl wherein up to three C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; R2 is selected from H, Me, Et, Pr and OH, each R2 being independently selected from H, Me, Et, Pr and OH when n is greater than 1; R3 (when n is 1) is selected from H, Me, Et and Pr; or (when n is greater than 1) each R3 is independently selected from H, Me, Et and Pr, or two R3 groups on neighbouring carbon atoms are linked to form a C3 to C6 carbocylic ring, or two R3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R2 and R3 on the same carbon atom together represent an ═O group; R4 is C1 to C15 hydrocarbyl wherein up to two C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; V is —CO—NH—SO2—Ph, —SO2—NH—CO—PH, —CH2OH, or a group of the formula —R7U, (wherein U is —COOH, tetrazolyl, —CONHOH or —SO3H; and R7 is a bond; C1 to C6 hydrocarbylene optionally substituted by hydroxy, amino or acetamido; —O—(C1 to C3 alkylene)—; —SO2NR8—CHR9—; —CO—NR8—CHR9—, R8 and R9 being independently selected from H and methyl; or —NH—(CO)c—CH2, c being 0 or 1); or a pharmaceutically acceptable salt thereof. Compositions comprising a compound a formula (I) are also described
WO2013148219A1 Anti-metatstatic agents predicated upon polyamine-macrocyclic conjugates Disclosed herein are novel motuporamine compounds that act as anti-metastatic agents with low toxicity and high anti-migration activity. The non-toxic, anti-metastatic agents may be given to patients with potential or actual metastatic cancers, such as pancreatic cancers, alone in combination with known and/or new therapies to help block the growth and spread of tumor(s)..
CN103204842A Crystalline Ilaprazole sodium hydrate and preparation method thereof The invention provides a crystalline Ilaprazole sodium hydrate and a preparation method thereof. An X ray powder diffraction spectrum of the crystalline Ilaprazole sodium hydrate provided by the invention includes diffraction peaks represented by the following 2 theta angles: 5.9 degrees +/- 0.1 degree, 25.4 degrees +/- 0.1 degree and 10.7 degrees +/- 0.1degree. The crystalline Ilaprazole sodium hydrate provided in the invention has high crystal purity. In addition, the method provided in the invention for preparation of the crystalline Ilaprazole sodium hydrate has the advantages of simple operation, mild reaction conditions, easy control, low production cost, definite obtaining of a target product crystal with good repeatability, less introduction of impurities, and significantly improves drug bioavailability.
US20080311181 Serum-Stable Amphoteric Liposomes The invention relates to amphoteric liposomal formulations which are provided with great serum stability and are suitable for the intracellular delivery of oligonucleotides.
CN101259101B Micrometre level arachidonic acid/docosahexaenoic acid emulsion and preparation thereof The invention discloses an emulsion of micron-sized arachidonic acid (ARA)/docosahexenoic acid (DHA) and a preparation method thereof. The emulsion comprises 50g to 150g of ARA and DHA (the ratio of ARA to DHA is 2 to 4), 10g to 100g of oil phase emulsifier, 0.1g to 10g of antioxidant, 5g to 40g of aqueous phase emulsifier, 100g to 300g of thickening and stabilizing agent and 10g to 100g of dispersant; water is added until the solution is 1000g. The emulsion of the invention is O/W type and mainly characterized in that the emulsifiers and the thickening and stabilizing agent are emulsified with the ARA/DHA and water according to certain proportions so as to obtain the emulsion with stable status and emulsified particle diameter less than 1 micron. The invention aims at providing a prescription of an ARA/DHA emulsion which is reasonable in nutrition-allocated proportion and capable of dispersing in cold water, provided with good stability and is stable against light, heat and oxygen andcan be conveniently used in beverage and other relevant industries.
WO2009094563A3 Crystalline form of calcium-salts of (3s)-aminomethyl-b-methyl-hexanoic acids and methods of use A crystalline form of Ca-salts of (3S) -aminomethyl-5-hexanoic acids and methods of preparing a crystalline form of a (3S) -aminomethyl-5-hexanoic acid and methods of using a crystalline form of a (3S) -aminomethyl-5-hexanoic acid are provided.
US20100249090 Neurotherapeutic composition and method therefor Neurotherapeutically effective pharmaceutical compositions are described that include carboxypeptidase E inhibitors. One class of carboxypeptidase E inhibitors found to exhibit significant neurotropic activity are β-lactam compounds, particularly penam and cephem β-lactam antibiotics and non-antibiotic derivatives thereof.
CN1771975A Total asiaticoside gel and its prepn The present invention provides one kind of total asiaticoside gel and its preparation process. The total asiaticoside gel of the present invention is prepared into compound transdermal promoter with high transdermal effect, high pharmacological effect and wide applicability. The present invention solves the problem of total asiaticoside, which has relatively great molecular weight and hard in transdermal absorption.
CN101352437A Use of amaryllidaceae alkaloid as tumour anti-apoptosis factor Mc1-1 inhibitor The invention belongs to the field of medicine, which relates to the application of Lycoris radiate alkaloid that is taken as tumor anti-apoptosis factor Mcl-1(myeloid cell leukemia-1) inhibitor, by inhibiting the protein expression of the tumor anti-apoptosis factor Mcl-1(myeloid cell leukemia-1), the diseases that are caused by the protein expression exception of Mcl-1, such as autoimmune inflammations, tumors, and the like, can be cured.
US7307080 Nuclear enzyme poly(adenosine 5'-diphospho-ribose) polymerase inhibitors; protection against ill effects of reactive free radicals and nitric oxide The disclosure relates to compounds, pharmaceutical compositions and methods for inhibiting PARP by use of the disclosed compositions. The compounds of the disclosure have the following structures I, II and III:
CN1853614A Decoloring method and decoloring agent for quinolone injection A decolorant for decoloring quinolione injection contains carbon powder and talc powder in weight ratio of 1: (2-6). Its coloring method includes such steps as heating the quinolione injection to 30-40 deg.C, proportionally adding carbon powder and talc powder, stirring for 15-60 min, and filtering.
US20090163458 Compositions and methods for treating Parkinson's disease and related disorders The present disclosure relates generally to methods and compositions for treating symptoms of Parkinson's disease and/or other movement disorders. More particularly, the present disclosure describes a method for treating symptoms of Parkinson's disease and related disorders by administering a composition comprising one or more of the following active agents; estradiol, estriol, testosterone, and 19-nortestosterone. In addition, the compositions of the present invention can be used for enhancing or optimizing the effectiveness of neural stimulation in treating the symptoms of movement disorders such as Parkinson's disease.
USRE42802 Phenylethylamines and condensed rings variants as prodrugs of catecholamines, and their use Compounds of the general formula I wherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings B, C and E being aliphatic whereas ring D may be aliphatic or aromatic/heteroaromatic, and wherein X is —(CH2)m—, in which m is an integer 1-3, to form a ring E or, when E is absent, a group R1 bound to the nitrogen atom, wherein R1 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 3 carbon atoms, cycloalkyl(alkyl) groups of 3 to 5 carbon atoms (i.e. including cyclopropyl, cyclopropylmethyl, cyclobutyl and cyclobutylmethyl) and wherein Y is —(CH2)n—, in which n is an integer 1-3, to form a ring C or when C is absent, a group R2 bound to the nitrogen atom, wherein R2 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 7 carbon atoms, cycloalkyl(alkyl) groups of 3 to 7 carbon atoms, alkenyl or alkylnyl groups of 3 to 6 carbon atoms, arylalkyl, heteroarylalkyl having 1 to 3 carbon atoms in the alkyl moiety, whilst the aryl/heteroaryl nucleus may be substituted, provided that when rings B, C, D and E are absent NR1R2 is different from dimethylamino, N-methyl-N-ethylamino, N-methyl-N-propynyl-amino, N-methyl-N-propylamino and N-hydroxipropyl-N-methylamino, and salts thereof with pharmaceutically acceptable acids or bases are disclosed as well as the use of such compounds for the manufacturing of pharmaceutical compositions for the treatment of Parkinson's disease, psychoses, Huntington's disease, impotence, renal failure, heart failure or hypertension, such pharmaceutical compositions and methods of treating Parkinson's disease and schizophrenia.
US20070141619 Drug resistance-associated gene and use thereof The present invention relates to a protein which excretes cancer chemotherapeutic drugs from a cell and which confers drug-resistance on the cell, a DNA encoding the protein, a method for detecting a cell type resistant to cancer chemotherapeutic drugs, a method for screening an inhibitor to overcome the resistance to cancer chemotherapeutic drugs as well as utilizing this knowledge to improve the therapeutic treatment of cancer patients.
CN102172261A Composition for constructing animal model of diabetes mellitus type II The invention provides a composition for constructing an animal model of diabetes mellitus type II and application of the composition to preparing feeds or drugs for constructing the animal model of the diabetes mellitus type II, wherein the composition comprises a conjugated linoleic acid mixture of which the weight percentage is more than 0.1% relative to the composition; and the animal model of the diabetes mellitus type II is prepared by feeding the composition to the mouse. Because the conjugated linoleic acid mixture or a single conjugated linoleic acid monomer is adopted as an inducer and the mouse is adopted as the animal protomodel, compared with a traditional chemical drug or diet induced animal model of the diabetes mellitus type II, the composition provided by the invention has the advantages of low price, convenience and easiness for raw material obtaining; and because the model establishing time is 4-6 weeks, the period is short, the formed model is characterized by hyperglycemia, high insulin level and in-vivo insulin resistance, the composition accords with basic characteristics of the diabetes mellitus type II and is an ideal composition for constructing the animal model of the diabetes mellitus type II.
EP1714658A1 Dietary supplement comprising antioxidant agents and carnitine or a precursor thereof, to be used as an aid to fertility in men and women Food compliment comprises: (a) a mixture of antioxidants and energizers comprising vitamin C and E, co-enzyme Q10 and/or vitamins B2, B5, B6, B9, B12, zinc salts/complexes, glutathione or lactoferrin, superoxide dismutase, selenium and unsaturated fats; (b) a mixture of energizers comprising carnitine and/or products capable of endogenous synthesis of carnitine, and magnesium. - ACTIVITY : Anti-abortive. No biological data given. - MECHANISM OF ACTION : None given.
US20060024307 For treatment and prevention of acute and chronic infectious diseases, mostly of viral etiology, and for producing an immunomodulating effect; comprising a homeopathically potentised form of monoclonal, polyclonal, or natural antibody to gamma interferon, does not suppress the activity of the interferon A medicament based on antibodies contains an activated form of monoclonal, polyclonal, or natural antibodies to interferon in low or ultra-low doses prepared by multiple consecutive dilutions and exposure to external factors, preferably in accordance with homeopathic technology. In order to obtain antibodies, human or heterologous interferon alpha, beta, or gamma, including recombinant interferon, is used; a mixture of various, mostly centimal, homeopathic dilutions being employed. A method of treating a pathologic syndrome, whose formation is affected by interferon, consists in the use of activated forms of antibodies to interferon alpha, beta, or gamma in low or ultra-low doses obtained by multiple consecutive dilutions and exposure to external factors.
WO2012137166A1 An oxoborolidine compound and uses thereof A boron-containing compound, 2-(4-fluorophenyl)-6-methyl-1,3,6,2- dioxazaborocane (Compound K), which exhibits antimicrobial and anti-biofilm formation activity, is provided, as well as methods and compositions using the same, either per se or in combination with an additional active agent, for inhibiting the grown of a pathogenic microorganism and/or for preventing and/or reducing the formation of microbial biofilms and/or for disrupting microbial biofilms in living tissues or inanimate objects.
EP2292600A1 Crystaline forms VI and VII of atorvastatin calcium The present invention relates to novel crystalline forms of atorvastatin calcium and to the methods of their production and isolation. More specifically, the present invention relates to novel Forms VI and VII of R-(R*, R*)]-2(4-fluorophenyl)-B, d dihydroxy-5(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1-H-pyrrole-1-heptanoic- acid calcium salt and hydrates thereof and to methods of their preparation.
WO2006028269A2 Thiazole derivatives having vap-1 ihibitory activity A compound of the formula (I): U-V-W-X-Y-Z (I) wherein U is lower alkyl; V is -CONH- or -NR1CO- wherein R1 is a hydrogen or lower alkyl; W is a bond or lower alkylene; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond or lower alkylene; and Z is a group of the formula: (a) wherein R2 is a group of the formula: -A-B-D-E-F-G wherein A is a bond or lower alkylene; B is a bond, (b); D is a bond, -CS- or -CO-; E is a bond or -NH-; F is a bond, -CO-, -O- or -SO2-; and G is lower alkyl, optionally protected amino, -OH, phenyl, (c); and R3 is lower alkyl, provided that when Z is a group of the formula: (d), then G should not be amino, when Z is a group of the formula: (e), then G should not be (f), when Z is a group of the formula: (g) and G is optionally protected amino, then D should be -CS-, or then A should be lower alkylene, B or E should be -NH- and F should be -CO-; or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor as well as a pharmaceutical composition and a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a subject, and the like.
US20110250272 Solid, orodispersible and/or dispersible composition, without an excipient of known effect and its process of preparation The present invention relates to a solid, orodispersible and/or dispersible composition comprising (a) from 0.1 to 59% by weight of at least one active substance with particle size no exceeding 50 μm; (b) from 40 to 99% by weight of at least one diluent without known effect, non water-soluble; (c) from 0.1 to 15% by weight of at least one disintegrating agent; and (d) from 0.05 to 10% by weight at least of one sweetening agent with particle size not exceeding 50 μm, percentages by weight being expressed compared to the total weight of the aforementioned composition. The present invention also relates to the use of said composition as a drug, a food supplement or in cosmetics and a method of preparation of an orodispersible and/or dispersible compound implementing said composition.
CN103006639A Application of aphanamixoid A in preparing antituberculosis medicament The invention discloses an application of aphanamixoid A in preparing an antituberculosis medicament. Regarding the current situation that the tuberculosis incidence rate and death rate are in a rising trend due to the high incidence rate of current tuberculosis and occurrence of multiple-resistant strain of mycobacterium tuberculosis, the invention discovers that aphanamixoid A has remarkable activity of inhibiting tuberculosis, and has a high application prospect. The application of aphanamixoid A in preparing a medicament for treating tuberculosis belongs to first disclosure, which has prominent substantial characteristics because the frame model belongs to a brand-new frame model, and has unexpectedly strong inhibiting activity to tuberculosis without the possibility of giving any revelation by other compounds, and the prevention and treatment of aphanamixoid A for tuberculosis infection has a remarkable progress.
WO2009071706A1 Pyrazolepyrimidine compounds useful for the treatment of degenerative & inflammatory diseases The present invention relates to compounds that are inhibitors of PDElA, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation, and particularly, to a compound according to formula I: or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof or isotopic variants thereof, stereoisomers or tautomers thereof. The invention extends to compositions, including pharmaceutical compositions, and corresponding uses thereof, and methods of prophylaxis and treatment involving the same.
CN101314579B Waterless Peramivir crystal and medicament composition thereof The invention relates to an anhydrous peramivir crystal compound and a preparation method thereof, and further discloses a pharmaceutical composition comprising the same and the application thereof in the preparation of medicaments for treating the influenza virus and the Avian influenza virus.
US20100035957 Methods for the Use of Inhibitors of Cytosolic Phospholipase A2 This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.
CA2801048A1 Antioxidant composition The present invention relates to an antioxidant composition that comprises a combination of galactomannan and N-acetylcysteine for use in the treatment of a skin disease or condition that is the result of the production of reactive oxygen species in the skin or that involves the production of reactive oxygen species in the skin. The invention also relates to a hydrogel containing said combination, to wound dressings that comprise said hydrogel, and to the use thereof in the healing of ulcers, wounds, burns and scalds.
CN101302243A 11-brominated-12-oleanane type pentacyclic triterpenoid and application thereof The invention provides an 11-bromo-12-olefin oleanane type pentacyclic triterpene compound, which has a structure as shown in formula (1). The compound has certain inhibition tumor cell growth activity, and can be used to make drugs for preventing and curing tumor diseases. Moreover, the compound has remarkable inhibition action on mice ear tumescence caused by toluene, and can be used to make anti-inflammatory agents. The structural general formula of the 11-bromo-12-olefin oleanane type pentacyclic triterpene compound as shown in formula (1) is shown in the graph.
US20090041757 Bone morphogenetic protein antagonist and uses thereof The present invention relates to the use of proteins that are differentially expressed in tumor associated stromal cells, as compared to normal stromal, as biomolecular targets for tumor treatment therapies. The present invention also provides compounds and pharmaceutically acceptable compositions for administration in the methods of the invention.
EP1557164A1 Adhesive patch containing tulobuterol A patch containing tulobuterol in the low concentration and having the stable release-controllability, prepared by laminating an adhesive layer consisting of a rubber, an adhesive resin and a plasticizer on a backing, wherein 1 to 4 w/w % of tulobuterol in the lower concentration as an active ingredient and 0.1 to 3 w/w % of a higher fatty acid as a drug-releasing controlling agent are contained in the adhesive layer.
US20100034749 Use of a Cationic Collodal Preparation for the Diagnosis and Treatment of Ocular Diseases The present invention relates to cationic colloidal preparations and their use for the diagnosis and/or treatment of ocular diseases.
US20100239668 Segmented pharmaceutical dosage forms Described is a layered or segmented controlled release pharmaceutical tablet adapted for separating one segment from another by breaking through a segment.
WO2014084433A1 Composition comprising peroxisome proliferator-activated receptor delta agonist, as active ingredient, for promoting treatment of myocardial injury after myocardial infraction The present invention provides a composition comprising (PPAR) peroxisome proliferator-activated receptor (PPAR) delta agonist, as an active ingredient, for promoting a treatment of a myocardial injury after a myocardial infraction so as to prevent and treat cardiovascular diseases.
EP2668179A1 New 5-alkynyl-pyridines 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.
US20100305159 Crystalline form of piperidine compound The present invention is to provide a crystalline form of (2R,4S)-1-{N-(3,5-bistrifluoromethylbenzyl)-N-methyl}aminocarbonyl-2-(4-fluoro-2-methylphenyl)-4-(2-hydroxyethylaminocarbonyloxy)piperidine or a solvate thereof.
CN101095692A Diet pill took orally The invention relates to oral fat-reducing pill, especially relates to a kidn of fat-reducing pill produced with edible liquid detergent and starch. The pill is taken with warm water, and the fat and fatty oil are removed by pill and discharged out together with fecal.
US7229983 antibacterial; beta -lactam antibiotics The present invention relates to novel, low molecular weight broad spectrum compounds in particular to a class of 4-substituted or unsubstituted-7-hydro-1,4-thiazepine-7-[bicyclic or tricyclic heteroaryl] substituted-3,6-dicarboxylic acid or their derivatives which have β-lactamase inhibitory and antibacterial properties. The compounds are therefore useful in the treatment of antibacterial infections in humans or animals, either alone or in combination with other antibiotics.
CN102101864A Trigonolactone A-D and medicinal composition, preparation method and application thereof The invention provides Trigonolactone A-D shown as a structural formula (I). The Trigonolactone A-D is macrocyclic diterpenoids with a novel chemical structure has remarkable HIV-1 (Human Immunodeficiency Virus 1) induction C8166 cell formation synplasm suppression activity, has the therapeutic index (TI) of between 1848 and 13484, and can be taken as an anti-human immunodeficiency virus (HIV) drug. In Trigonostelliimone A(1), R1 is Cl; and R2 is H; and in HTrigonostelliimone B(2), R1 is H and R2 is H.
WO2009083270A1 15,16-methylene-steroid-17,17-lactol derivative, use thereof, and medicament containing said derivative The invention relates to (15, 16)-methylene-steroid-(17, 17)-lactol-derivates with general chemical formula (I) and the tautomer forms thereof with general chemical formula (Ia) wherein R4, R6a, R6b, R7, R18, R22 and Z have the designations given in claim 1, and to the solvates, hydrates, stereoisomers and salts thereof. The invention also relates to the use of said derivatives for producing a medicament for oral contraception and for the treatment of premenopausal, perimenopausal and postmenopausal troubles, and medicaments containing said derivatives. The derivatives according to the invention have a gestagen effect, and in preferred cases, also an anti-mineral corticoid and neutral to lightly androgenous effect.
CN103271928A Prescription technique for improving stability of desogestrel The invention discloses a prescription technique for improving the stability of desogestrel. According to the prescription technique, active medicines of the prescription are dissolved in a solvent mixture of which the weight is 5-200 times the weight of the active medicine; the active medicines are desogestrel and ethinylestradiol; the solvent mixture is chloroform or other solvent mixtures; and the active medicines are completely dissolved in the solvent mixture, and then an antioxygen of which the amount is 2-10 times the amount of the active medicines is added; the antioxygen including vitamin C or vitamin E is dissolved, so that the active medicines and the antioxygen are a solution at molecular distribution state, and each active medicine molecule is surrounded and protected by a plurality of antioxygen molecules. The prescription technique disclosed by the invention improves the stability of main medicines of the oral contraceptive and has the advantage that the shelf time of the oral contraceptive consisting of desogestrel and ethinylestradiol is as long as 24 months, etc.
US20090239860 Novel benzofuran derivative, medicinal composition containing the same, and uses of these The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, aryl, aralkyl, arylalkenyl, aryloxy-lower alkyl, heteroaryl, heteroaryl-lower alkyl, etc; R3, R4, R5 and R6 are each hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, lower alkoxy, hydroxy, aryl, etc; provided that at least one of R3, R4, R5 and R6 is other than hydrogen. Compound (I) of the present invention shows a potent adenosine A2A receptor antagonistic activity, and are useful for treating or preventing a disease mediated by adenosine A2A receptors such as motor function disorders, depression, anxiety disorders, cognitive function disorders, cerebral ischemia disorders, restless legs syndrome and the like.
US20080153915 Pharmaceutical Preparation For the Oral Cavity A throat, mouth and/or gum sprayable pharmaceutical preparation in the form of an aqueous solution. One embodiment of such a solution may comprise: a non-steroidal anti-inflammatory drug (NSAID) also having analgesic activity; a biologically compatible buffer consisting essentially of an organic amine selected from at least one D-glucamine, meglumine, trometamol (tris buffer) and a mixture thereof, in a quantity suitable for buffering the pH of the preparation within the range of between about 6.5 and about 8.0; and pharmaceutical grade water; wherein the NSAID is flurbiprofen.
CN1969984B Externally applied medicament for treating acne and allergy The invention discloses an externally-used medicament for treating skin acne and allergy which is prepared from the following raw materials (by weight portion): rheum officinale 10-20 parts, honeysuckle flower 5-15 parts, baikal skullcap root 5-15 parts, buthus martensi kirsch 5-15 parts, cordate houttuynia 5-15 parts, root of Dahurain angelica 5-15 parts, kuh-seng 5-15 parts, Chinese dittany bark 5-15 parts and borneol 2-5 parts. The preparing process consists of steps of disintegrating the raw materials to 50-100 meshes, charging distilled water and preservative agent for immersion.
CN102846686A Novel liquid vitamin for breeding hen or laying hen and preparation method of novel liquid vitamin The invention provides a novel liquid vitamin for a breeding hen or a laying hen and a preparation method of the novel liquid vitamin. The liquid vitamin is prepared from the following components in parts by weight: 0.005-0.01 part of sodium pyrosulfite, 0.2-0.8 part of vitamin C, 0.2-0.4 part of vitamin B1, 0.1-0.3 part of vitamin B6, 0.2-0.5 part of calcium pantothenate, 0.04-009 part of vitamin K, 0.05-0.12 part of carnitine, 0.05-009 part of compound amino acid, 5-10 parts of sorbitol, 0.02-0.05 part of BHT (Butylated Hydroxytoluene), 0.1-0.3 part of sodium benzoate, 9-15 parts of Tween80, 10-15 parts of propylene glycol, 0.3-0.9 part of vitamin A, 0.2-0.4 part of vitamin E, 0.005-0.01 part of vitamin D, 0.2-0.8 part of ginseng stem and leaf saponins and 50-70 parts of injection water.
US20120201874 Liposome Having Inner Water Phase Containing Sulfobutyl Ether Cyclodextrin Salt A liposome comprising bilayer and inner water phase is disclosed. Said inner water phase contains sulfobutyl ether cyclodextrin and active compound. Said sulfobutyl ether cyclodextrin is sulfobutyl ether α-cyclodextrin, sulfobutyl ether β-cyclodextrin, or sulfobutyl ether γ-cyclodextrin.
WO2004009026A8 Cholinergic therapy for individuals with learning disabilities Cholinergic agents are used to improve specific learning deficits and language function in individuals of normal intelligence. Psychosocial deficits including a pragmatics impairment, reading deficits, a problem solving impairment, an information processing impairment, an adaptive function impairment, social skills impairment, attention impairment, a mood impairment and employment skills impairment, can also be treated in this manner. The cholinergic treatments can be combined with more traditional educational, psychological, and behavioral therapies for enhanced therapeutic benefit.
CN101596263A Medicine for treating fracture and preparation method thereof The invention discloses a medicine for treating fracture and preparation method thereof. Clove, costustoot, sanguis draconis, native copper, prepared rhizome of rehmannia, rhubarb, angelica, safflower, ginseng, teasel root, drynaria rhizome, liquorice and honey are mixed by ratio, ground into fine powder and refined into pills. The invention has efficacies of activating bland circulation to dissipate blood stasis and promoting circulation of qi and to relieve pain and has excellent curative effect of treating injuries from falls, contusions and sprain, fracture, injury of tissues and the like. Compared with self healing, the healing time can be advanced for 15-20 days.
US7253154 Substituted thiazolopyrimidines as xanthine oxidase inhibitors The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which may have a substituent or the like; R2 is halogen, nitro, cyano, carboxyl, or the like; R3 is hydrogen, halogen, hydroxyl, amino, carboxyl, or the like; X is NR11, oxygen, or sulfur, in which R11 is hydrogen, or an alkyl group having 1-8 carbon atom which may have a substituent; and each of Y and Z is CR12 or nitrogen, in which R12 has the same meaning as R3 above, and a xanthine oxidase inhibitor containing the compound as an active ingredient.
WO2011052950A3 Pharmaceutical composition comprising indole compound The present invention relates to a pharmaceutical composition comprising a compound of formula (1), (2) or (3) as defined in the specification for the prevention or treatment of diseases associated with oxidative stress, mitochondria dysfunction, hypoxic injury, necrosis and/or ischemic reperfusion injury, and a cosmetic composition comprising an indole compound having an antioxidant effect.
US20060257843 Kappa-PVIIA-related conotoxins as organ protectants The invention relates to κ-PVIIA-related conotoxins and their use as organ protecting agents, i.e., organ protectants. These conotoxins can be used for arresting, protecting or preserving an organ, such as a circulatory organ, a respiratory organ, a urinary organ, a digestive organ, a reproductive organ, an endocrine organ or a neurological organ. These conotoxins can also be used for arresting, protecting or preserving somatic cells.
CN1579448A Nasal spray for treating headache and hemicrania and its preparation method The invention relates to a nose cavity spraying agent for curing headache and migraine and its manufacutirng method. The prescription includes medicine effective ingredients and accessories, the effective ingredients of the medicine is made up of 1-10 shares of chuanxiong rhizome extract, asarum extract and mint extract, the extraction of the effective ingredient may be steam distilling extract method or supercritical fluid extraction method, then the accessories are dissolved in the solution waterless alcohol, then adds in the effective ingredients of each medicine, they are blended fully and poured into the nose cavity spraying pump, the nose cavity spraying agent uses the rich mucous and vessels in the nose cavity, the absorption of the medicine is quick, the biology utilization rate is high, the effect is prominent, and it has no propellant, it does not use pressure resisting container, the atomization drop is tiny, it is even in the nose cavity.
EP1689387B1 Bicyclic inhibitors of mek and methods of synthesis thereof Disclosed are compounds of the Formula (I) and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, R10, R20, R21, and R22 are as defined in the specification. Such compounds are MFK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
CN101229129A Ceftezole sodium powder injection and synthesizing method thereof The invention which provides a ceftezole sodium powder injection and a synthesis method for the powder injection consists of more stable ceftezole sodium crystals; in the method, tetrazoleacetic acid, N, N'- dicyclohexylcarbodiimide and 7-amino cefgadoleic acid with the proportion of 1.4 to 1.7:1 to 1.3:1 make reactions in dimethyl sulfoxide; ceftezole is prepared by causing a react intermediate to react with thiadiazole thiol of 1.1 to 1.3 times; the ceftezole sodium is prepared in sodium bicarbonate water solution after acetone is re-crystallized. The method is easy in operation and has the total yield of 55.5 percent.
WO2014160360A1 Tubulysin compounds and conjugates thereof A tubulysin compound conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by Lp. Each occurrence of D is independently a tubulysin compound having a molecular weight < 5 kDa. LD and Lp are distinct linkers connecting the tubulysin compound and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-tubulysin compound-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
CN101391005A Health-care medicinal wine capable of relaxing muscles and joints and promoting blood circulation The invention provides a health medicine wine for relieving rigidity of muscles and promoting blood circulation, which is composed of following active ingredient materials: lopseed, camphor, frankincense, myrrh, fructus psoraleae, safflower, uncaria, radix sileris, fructus liquidambaris, rhubarb, heracleum hemsleyanum michaux, pawpaw, radix aconiti, cattail pollen, sapanwood, red paeonia, cistanche salsa, achyranthes, blood resin, atractylodes, homalomena rhizome, tuckahoe, ephedra equisetina, asarum, radix cyathulae, clematis chinensis and white wine. The medicine wine can effectively improve stomach function and adjust the human body internal secretion, rectify the decompensation, regulate the viscera, adjust the ying and yang balance, promote the blood cycle, enrich yin and nourish kidney so as to improve the human body immunity function and delay consenescence; using the medicine wine can also rapidly cure the diseases such as periarthritis humeroscapularis, cervical spondylosis, lumbar intervertebral disc protrusion, sciatica, rheumatism, rheumatoid disease and caput femoris necrosis; the medicine wine can realize the purpose of curing various diseases with one medicine, and can reach the heath care effect at the same time.
CA2569428A1 Methods and devices for treating vulnerable plaque This invention provides methods, devices and kits for treating coronary artery disease, particularly "soft" or vulnerable plaque. The invention is based on the local delivery of crosslinking means to crosslink the collagen covering the plaque and other proteins that may be present at the site to stabilize the plaque and prevent leakage of thrombogenic material into the lumen of the coronary artery. In certain embodiments, catheters are employed to achieve local delivery of a crosslinking agent or ultraviolet light.
US20110064798 Suspension containing hydronium stabilized colloidal silicic acid nanoparticles, formulation obtained from the said dilutesuspension, powder obtained from the said de-hydrated suspension, compositions obtained from the said powder, preparation and use The present invention relates to hydronium stabilized silicic acid nanoparticles, to the formulation obtained from the said diluted suspension, to the powder obtained from the said dehydrated suspension and to the preparation or dosage form obtained from the said suspension, formulation or powder, to their preparation and their use in all kinds of applications in the domains of food, medicine, pharmaceutics, cosmetics. The present invention provides a stable suspension of colloidal silicic acid nanoparticles having a pH lower than 0.9, a molar silicon concentration between 0.035 and 0.65, a free water concentration of at least 30% (w/v) and a ratio between hydronium ion and Si molar concentrations higher than 2 and preferably inferior to 4. The present invention further provides a method for preparing a stable suspension of colloidal silicic acid nanoparticles, which comprises the steps of providing an aqueous inorganic or organic silicon solution and quick mixing said aqueous inorganic or organic silicon solution with water containing a strong acidic compound at a temperature inferior at 30° C., preferably comprised between 1 and 25° C., to form a suspension of colloidal silicic acid nanoparticles having a pH lower than 0.9, stabilized by hydronium ions, the ratio between hydronium ions and Si molar concentrations being higher than 2 and preferably inferior to 4, for a molar silicon concentration between 0.035 and 0.65 and a free water concentration of at least 30% (w/v).
CA2238864C Method for the synthesis of a benzimidazole compound A process for the manufacture of omeprazole from pyrmethyl alcohol via pyrmethyl chloride and pyrmetazole characterized in that the whole reaction sequence is carried out without any isolation or purification of intermediates. Further that the reaction is carried out in a main solvent system common for the whole reaction sequence and inert to the reactants formed during the process and used in the process. The process according to the present invention may also include an additional purification step. Omeprazole has the structure:(see above formula)
US8580791 Antiviral 6-{2-[1-(6-methyl-3-pyridazinyl)-4-piperidinyl]ethoxy}-3-ethoxy-1,2-benzisoxazole bis-dihydrogen-phosphate salts Novel acid addition salts of 6-{2-[1-(6-methyl-3-pyridazinyl)-4-piperidinyl]ethoxy}-3-ethoxy-1,2-benzisoxazole of following formula are disclosed, particularly a crystalline form of a bis-dihydrogenphosphate salt: Such compounds have particular advantages with regard to treatment of picornaviruses. Related pharmaceutical compositions and methods of treating a picornavirus infection are also disclosed.
US20090214552 Novel Egg Receptors for Sperm Proteins The present invention relates to novel egg membrane protein receptors and to methods of inhibiting the interaction of sperm proteins with egg proteins. The invention further relates to methods of preventing and inhibiting sperm-egg binding, sperm-egg fusion, and fertilization. The invention further relates to the egg membrane proteins MET and ZEP.
CN101890016A Piperacillin sodium-tazobactam sodium medicinal composition microsphere injection The invention discloses piperacillin sodium-tazobactam sodium medicinal composition microsphere injection. The injection is characterized by consisting of piperacillin sodium, tazobactam sodium, polylactic acid-polyethylene glycol (PLA-PEG), PEG600, polysorbate 80 and mannitol and particularly consisting of 4 to 8 parts of piperacillin sodium, 1 part of tazobactam sodium, 4 to 9 parts of PLA-PEG, 6 to 10 parts of PEG600, 1 to 3 parts of polysorbate 80 and 2 to 4 parts of mannitol. Compared with the prior art, the piperacillin sodium-tazobactam sodium medicinal composition microsphere injection prepared by the invention has the characteristics of good stability, high entrapment rate, high preparation technology repeatability, suitability for industrial production, uniform particle distribution, few solvent residue, good injectability and excellent sustained release property.
WO2006064189A1 Oxadiazole derivatives as dgat inhibitors Compounds of formula (I), and salts and pro-drugs thereof: Formula (I) wherein for example R1 is optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.
CN102366406A Salmeterol/fluticasone aerosol preparation with hydrofluoroalkane as propellent The invention discloses a salmeterol/fluticasone aerosol preparation with hydrofluoroalkane as a propellent. The salmeterol/fluticasone aerosol preparation contains salmeterol or salmeterol/fluticasone propionate or their pharmaceutically acceptable salt or solvate and a hydrofluoroalkane propellent which are effective in treatment or prevention, wherein salmeterol or fluticasone propionate or their pharmaceutically acceptable salt or solvate is a particle medicine. The aerosol provided by the invention is a medical aerosol preparation with good stability. One-step or two-step canning method is used during the technological process.
US20050261378 Process for decreasing adiposity using vitamin A as a dietary supplement A process is provided for reducing adiposity in an animal such as a companion animal by feeding the animal an effective amount of Vitamin A for a time sufficient to reduce adiposity in the animal. Preferably, the such effective amount comprises from about 50,000 IU to about 1,000,000 IU of Vitamin A per kilogram of diet. Such an effective amount provides sufficient Vitamin A to decrease accumulation of body fat, increase UCP1 levels, and decrease serum leptin levels in the animal.
EP1176969B1 Substitution infusion fluid and citrate anticoagulation The invention relates to a substitution infusion fluid for hemofiltration of a specific composition. The use of said substitution infusion fluid significantly reduces the risk of the occurrence of abnormalities in a patient undergoing hemofiltration. The invention also relates to a process for hemofiltration of blood wherein said substitution infusion fluid is used. The invention also relates to a citrate anticoagulation fluid of a specific composition. The invention also relates to a process for hemofiltration of blood wherein said substitution infusion fluid is used in combination with said citrate anticoagulation fluid. The use of said substitution infusion fluid in combination with said citrate anticoagulation fluid significantly further reduces the risk of the occurrence of abnormalities in a patient undergoing hemofiltration.
CN102028850A Specific ointment for treating chilblain The invention discloses a specific ointment for treating chilblain, which comprises the following components in part by weight: 10 to 25 parts of Szechuan lovage rhizome, 15 to 25 parts of camphor, 5 to 15 parts of borneol, 15 to 30 parts of prepared common monkshood daughter root, 5 to 10 parts of cassia bark, 10 to 32 parts of Sinkiang arnebia root, 1,000 to 2,500 parts of sesame oil, 5 to 15 parts of root of red-rooted salvia, 12 to 26 parts of aloe vera gel, 10 to 25 parts of safflower, 15 to 25 parts of notoginseng root, 10 to 20 parts of nutgrass galingale rhizome and 60 to 100 parts of yellow wax. The specific ointment has low medicinal cost, is wide in raw material sources, contains high-energy components for activating blood and dissolving stasis, can effectively improve microcirculation, increase epidermal metabolism, expand blood vessels and release cold, can relieve the swelling, fever and pruritus symptoms of skin suffering from the chilblain, has the effects of converging, diminishing inflammation and relieving pain, can clear fester, detoxify and promote tissue regeneration when applied to a wound, has good anti-infection effect and a short treatment period, does not cause pain, and greatly improves the cure rate of patients with the chilblain; and color lump spots or atrophic scars are not left on the skin after the chilblain is cured, and the chilblain cannot be relapsed after being cured.
EP1645272A2 Daidzin derivatives for the treatment of alcohol dependence or alcohol abuse A method for the treatment of alcohol abuse using diadzin and compounds analogous to diadszin is disclosed. Also disclosed is a method for screening compounds having antidipsotropic activity.
WO2006127909A2 Polymorphic forms of (s)-1-cyanobutan-2-yl (s)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl) phenyl) ureido) phenyl) ethylcarbamate The present invention relates to polymorphic forms of ( S ) -l-cyanobutan-2-yl ( S ) -1- ( 3 - ( 3 - ( 3 -methoxy-4- ( oxazol-5- yl ) phenyl ) urei do ) phenyl ) ethyl carbamate , pharmaceutical compositions thereof , processes to prepare therein, and uses therewith .
EP2673279A1 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I); wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X and Y of Formula (I) are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas (II) and sub-formula embodiments of Formula (I) and (II), intermediates and processes and methods useful for the preparation of compounds of Formulas (I)-(II).
US20090258908 Crystalline S-Omeprazole Strontium Hydrate, Method For Preparing Same, And Pharmaceutical Composition Containing Same This invention provides a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.
US20100172933 Recombinant vectors based on the modified vaccinia ankara (mva) virus as vaccines against lieshmaniasis The invention relates to recombinant vectors based on the Modified Vaccinia Ankara (MVA) virus as vaccines against leishmaniasis. The inventive vectors contain sequences encoding the LACK protein, which are preferably inserted into the hemagglutinin locus of the virus under the control of a promoter, which enables the expression of same throughout the infection cycle of the virus. The invention comprises stable, safe vectors which elicit a strong immune response that provides protection against leishmaniasis and which, as such, are particularly suitable for use in vaccination against said disease, especially in humans, s well as in the largest animal reservoir of said anthropozoonosis, i.e. dogs.
WO2005117852A1 Composition for treatment of a hydrofluoric acid burn The present invention provides a composition for the treatment of a hydrofluoric acid burn. The composition comprises a non-toxic calcium compound, for example a non-toxic organic calcium compound such as calcium levulinate, in a carrier, such as water, an aqueous dimethyl sulphoxide solution, or an aqueous urea solution. When applied to an affected area, calcium ions react with fluoride ions, thereby neutralizing the fluoride ions and preventing further damage to the skin tissue in or on the affected area.
US20120301520 Directly compressible magnesium hydroxide carbonate The present invention relates to a directly compressible magnesium hydroxide carbonate and to a process for the preparation thereof, and to the use thereof.
WO2010053835A1 Compositions and methods for minimizing or reversing agonist-induced desensitization Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.
CN101897839B Comprehensive utilization method of banana stalks The invention provides a comprehensive utilization method of banana stalks, which comprises: preparing raw liquid of banana stalk juice by washing the banana stalks, crushing, screening, soaking, squeezing, filtering, blending and homogenizing; packaging or directly concentrating the raw liquid of the banana stalk juice; and refining for extracting active ingredients from tannin or preparing related antibacterial products. In the invention, the active ingredients of plant tannin are recovered, the problem of pollution caused by the stacking of a large amount of banana stalk waste one the edgeof a field is solved, the fibers in the banana stalks can be used for making paper, and the method has three purposes and is benefit for the state and people.
CN101601694A Preparation method of powder for healing furuncle The invention discloses a preparation method of a powder for healing furuncle in the technical field. The furuncle wound can be closed and healed within one day by using the method. The method is realized by adopting the following technical scheme that: pigeon manure is slightly stirred for 1-6 hours at 50-70 DEG C, white muscardine silkworm is fried, fish glue (fish bladder and clam powder) is fried for 50-90 minutes at 80 DEG C, the moisture content does not exceed 5 percent, the medicinal herbs are mixed together and processed into 300 meshes of fine powder and then added with realgar to be stirred in a mixed manner for 10 minutes to obtain the finished powder.
CN101066261B Application of dryopteris fragrans phloroglucinol extract The present invention discloses the application of Dryoptesis fragrass phloroglucinol extract in preparing medicine for treating tumor, especially in preparing medicine for treating S180 sarcoma, Lewis lung cancer and HepA liver cancer. Dryoptesis fragrass phloroglucinol extract from natural botanical resource has high antitumor activity and high safety. It is hopeful to discover new anticancer medicine with high selectivity, high activity, less toxic side effect, wide antitumor spectrum and drug tolerance resistance in further research on the extract.
CN101991594A Compound lincomycin hydrochloride injection and reparation method thereof The invention relates to compound lincomycin hydrochloride injection and a preparation method thereof. The preparation method comprises the following steps: (1) adding aminopyrine and prednisolone acetate into 95% ethanol and stirring for 10-25 min until the solution is clear; (2) fetching 300 L of injection water, adding kanamycin sulfate and lincomycin hydrochloride in turn and stirring for dissolution; and (3) mixing the solutions obtained in steps (1) and (2), adding injection water until the solution volume is 1,000 L, uniformly stirring and maintaining for 15-20 min until the liquid medicine is clear to obtain the compound lincomycin hydrochloride injection. The invention has the advantages that the compound preparation of kanamycin sulfate and lincomycin hydrochloride, the aminopyrine with adjuvant therapy effect and prednisolone acetate with adjuvant therapy effect are adopted and combined for use, thus achieving antibacterial action on gram-negative bacteria and gram-positive bacteria due to the joint application of the four medicines; and the antimicrobial spectrum is wide, the antimicrobial range is expanded, pig paratyphus and certain complications can be comprehensively treated, the curative effect is good and quick, the drug resistance rate of bacteria is reduced and the curative effect is enhanced.
EP1675557A1 Composition comprising a sesquiterpene lactone The present invention relates to a pharmaceutical, dermatological or cosmetic composition, comprising, as an active agent, at least one sesquiterpene lactone, or a derivative or analog thereof, or at least one plant extract, containing at least one sesquiterpene lactone. Advantageously, said sesquiterpene lactone is vulgarin.
CA2547617C Amide derivatives bearing a cyclopropylaminoacarbonyl substituent useful as cytokine inhibitors This invention relates to amide derivatives of Formula I, or pharmaceutically-acceptable salts thereof, which are useful as inhibitors of cytokine mediated diseases. The invention also relates to processes for the manufacture of said amide derivatives, to pharmaceutical compositions containing said amide derivatives and to their use in therapeutic methods, for example by virtue of inhibition of cytokine mediated disease. (see formula I)
US20050131027 Fine particle size pioglitazone The present invention provides pioglitazone of defined particle size distribution. The Pioglitazone of defined particle size can be formulated into a wide variety of dosage forms.
WO2008102372A1 A composition derived from fenugreek for improving physiology The present invention relates to a novel herbal composition for improving exercise physiology factors comprising saponins and sugar derivatives optionally along with pharmaceutically acceptable excipients. It also relates to the process of preparing the composition for improving exercise physiology factors comprising the steps of flaking, defatting, solvent extraction of seeds of trigonella species followed by concentration of the extract to obtain a saponin and sugar derivative. It also relates to the use of the composition for improving exercise physiology factors comprising, enhanced anabolic activity, enhanced muscle building, enhance creatine delivery and reuptake, an increase in testosterone levels and an enhanced immunity.
US20120129916 Cell-targeting nanoparticles comprising polynucleotide agents and uses thereof A method of generating a particle is disclosed, the particle being for delivery of a polynucleotide to a target cell. The method comprises (a) contacting the polynucleotide with a composition comprising cationic molecules, wherein the cationic molecules condense the polynucleotide by electrostatic interactions to generate a complex, wherein the cationic molecules are not comprised in a liposome; and (b) covalently binding the complex to a targeting moiety at a pH equal to or below about 4.5, thereby generating the particle for delivery of the polynucleotide agent to the target cell. Use of the particles and compositions comprising same are also disclosed.
WO2014117919A1 Positive allosteric modulators of mglur3 The present invention relates to novel substituted pyridine derivatives as positive allosteric modulators for modulating metabotropic giutamate receptor subtype 3 (mGluR3) and/or altering giutamate level or glutamatergic signalling.
US20070243260 Treatment of Childhood Asthma Glycopyrrolate or an analogue thereof is useful for the treatment of childhood asthma.
EP1341786B9 Substituted derivatives of aminofuran-2-yl-acetic acid and aminothien-2-yl-acetic acid and the use thereof for treating migraines and pain The invention relates to substituted aminofuran-2-yl-acetic acid derivatives and substituted aminothien-2-yl-acetic acid derivatives of general formulae (I-A) and (I-B). The invention also relates to a method for the production thereof, medicaments containing the same, the use of said compounds for producing medicaments for treating, inter alia, pain and migraines, and pharmaceutical compositions containing the same.
US20080213189 Multifunctional metal-graphite nanocrystals Disclosed are nanocrystals comprising metals and metal alloys, which are formed by a process that results in a layer of graphite in direct contact with the metallic core. The nanocrystals may be used in vivo as MRI contrast agents, X-ray contrast agents, near IR (NIR) heating agents, drug delivery, protein separation, catalysis etc. The nanocrystals may be further functionalized with a hydrophilic coating, e.g., phospholipid-polyethylene glycol, which improves in vivo stability. The process comprises chemical vapor deposition of metals adsorbed onto silica as a fine powder, in conjunction with a carbon containing gas, which coats the metal particles. The silica is then etched away. Preferred metals include iron, gold, cobalt, platinum, ruthenium and mixtures thereof, e.g., FeCo and AuFe. The process permits control of the alloy compositions, size, and other characteristics.
CN101397295A 2-dihydroindolemanone derivates as histone deacetylase inhibitor, preparation method and use thereof The invention discloses 2-isatin derivatives, the preparation method and the application. The structure of the invention is shown as the formula (I), wherein, the definitions of R<1>, R<2>, R<3>, R<4>, R<5>, X, Ar and n are shown in the description of instruction. The compound is provided with the restraining activity against histone deacetylase so as to treat the diseases relevant to the abnormal condition of the histone deacetylase, including Rubinstein-Taybi II-syndrome, fragile x syndrome, leukemia, cancer, immunological diseases, cardiac hypertrophy, bone diseases, nervous system diseases and neurodegenerative diseases.
US20110223118 Antibacterial pharmaceutical composition comprising aceriphyllum rossii extract and active compounds isolated therefrom The present invention relates to an antibacterial pharmaceutical composition comprising an Aceriphyllum rossii extract, and aceriphyllic acid A and 3-oxo-12-oleanen-27-oic acid isolated therefrom. The Aceriphyllum rossii extract of the present invention, and aceriphyllic acid A and 3-oxo-12-oleanen-27-oic acid isolated therefrom have strong antibacterial activities against Staphylococcus aureus, methicillin-resistant S. aureus, quinolone-resistant S. aureus, Acinetobacter calcoaceticus, Micrococcus luteus, Bacillus subtilis or Streptococcus mutans, Propionibacterium acnes, thereby being used for the prevention or treatment of pathogenic bacterial and resistant bacterial infections, cariogenic bacterial and acne bacterial infections.
CN101328228B Tang oligosaccharide, preparation thereof and use in radioresistant medicaments The invention relates to algae oligosaccharide, which is characterized in that: sugar chains of the algae oligosaccharide contain rhamnose groups, xylose groups, glucose groups, galactose groups, mannose groups and glucuronic acid groups; the weight percentage of sulphate groups in the algae oligosaccharide is between 10 and 40 percent; and molecular weight is between 3,000 and 10,000 daltons. Under the condition of preparation, algae frond is added with water for immersion and homogenate, and then heated and extracted, and a clear solution is separated, concentrated and desalinated; the desalinated solution is concentrated and deproteinized; the deproteinized solution is concentrated and added with acid or an oxidant, undergoes heating reaction and cooling reaction, and then is added with alkali for neutralization or added with an enzyme for reaction termination, and a clear solution is separated, concentrated, desalinated; the desalinated clear solution is concentrated and separatedby an ultrafiltration membrane; and the collected solution is desalinated, concentrated, dried and crushed. The algae oligosaccharide can be used for preparing a novel antiradiation drug.
US20050042171 Only once daily administration of an antispasmodic beta-2 adrenergic agonist and an antiinflammatory corticosteroid; inhalation; salmeterol xinafoate Methods for the prophylaxis or treatment of asthma by once daily administration of salmeterol and fluticasone propionate combinations as well as suitable pharmaceutical formulations are disclosed.
WO2007072965A1 Angiogenesis inhibitor and utilization of the same It is intended to provide a novel angiogenesis inhibitor. For achieve thus purpose, an angiogenesis inhibitor which contains a sulfated polysaccharide having rhamnose as the main constituting monosaccharide or its salt is provided.
CN103622930A Metformin hydrochloride slow release preparation and preparation method thereof The invention relates to a metformin hydrochloride slow release preparation and a preparation method thereof. The metformin hydrochloride slow release preparation comprises a core (1) and a slow release coating (2), wherein the core comprises 50-60% of metformin hydrochloride, 23-25% of filling agents, 4.5-8% of adhesives, 11-16% of absorption enhancer and 0-1% of lubricating agent; the slow release coating accounts for 8-12wt% of the core and comprises an acrylic macromolecule, a plasticizing agent, an anti-sticking agent and a pore-foaming agent in a weight proportion of 5:0.15:0.45:1. The invention also provides the preparation method of the slow release preparation. The slow release preparation can be used for solving the problems that metformin hydrochloride is subjected to burst release at the upper parts of gastrointestinal tracts and absorption windows are narrow, is released slowly within six hours, is released stably and can be effectively absorbed and utilized.
US20100273848 Iminopyrrolidone thiol amino acid conjugates, pharmaceutical compositions and methods for the treatment of cancer Compounds, compositions and methods for the treatment of cancer are disclosed herein. Embodiments of the present invention include compounds having the formula: (I), wherein R1 is selected from hydrogen or substituted or unsubstituted (C1-C6) alkyl or (C3-C6) cycloalkyl, R2 and R3 are independently selected from hydrogen, substituted or unsubstituted (C1-C6) alkyl, (C4-C6) cycloalkyl, or taken together with the N atom to which they are attached form a 3-6 membered heterocycloalkyl, and n is 1-5. Embodiments of the present invention also include pharmaceutical compositions comprising compounds of Formula (I) or pharmaceutically acceptable salts thereof, and methods of treating cancer via the administration of such compounds to patients in need of such treatment.
CN101200467A New compound generated by streptomycete and preparation method thereof The invention discloses a novel compound prepared from streptomyces and a preparation thereof. The invention utilizes the streptomyces albulus var.xuzhouensis CGMCC1815 as the producing strains. The streptomyces carries out the liquid fermentation in the culture medium containing the inorganic salt and vitamin to obtain the mycelium of the streptomyces, fermentation supernatant and various metabolites. The fermentation supernatant and the mycelium after fermentation are extracted by chloroform or ethanol, and the novel compound with the structural formula is obtained by the extracting separation and the purification. The novel compound has the anti-tumor activeness.
CN1840205A Transgene mouse model of poly glumine disease, its culturing method and medicine for treating the disease This invention relates to a kind of polyglutamine disease (DRPLA) transgenosis mouse model, culture method and drug for treating the disease. DRPLA is a nerve regression disease caused by glutamine's repeat sequence CAG expanding unconventionally. The invention establishes DRPLA transgenosis mouse model, achieves cultivate method of the model, and obtains a drug for curing the DRPLA disease, accordingly the intention of curing DRPLA disease is achieved.
US20110281899 Methods of preventing and treating low bone mass diseases The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.
CN103721034A Radix Ophiopogonis health liquor used for pharyngitis The invention relates to a Radix Ophiopogonis health liquor used for pharyngitis. The Radix Ophiopogonis health liquor is prepared through the steps of washing 18g of Radix Ophiopogonis, 11g of dragon's blood, 14g of licorice root, 14g of Achyranthes bidentata, 11g of borneol and 16g of Radix Scrophulariae, air-drying, grinding the above raw materials to powder, putting the powder in an extraction pot, adding a 48-54DEG white liquor having an amount 5 times the mass of the medicinal materials, immersing for 6-18 days, filtering to obtain a filtrate, adding 3500g of a pure grain liquor into the filtrate, and carrying out sealed storage for 1-2 months. The Radix Ophiopogonis health liquor used for pharyngitis has the advantages of simple preparation method, drinking convenience and good effect, has the efficacies of liver and kidney nourishing, heat clearing and throat disinhibiting, and can be frequently drunk to realize the liver and kidney nourishing, heat clearing and throat disinhibiting of people in order to alleviate symptoms of the pharyngitis.
EP1768667A1 Cannabinoid receptor ligands Compounds of Formula (I) and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be effective asCB2 receptor ligands in treating cancer and inflammatory, immunomodulatory or respiratory diseases or conditions.
CN102885852A Povidone iodine ointment and preparation method thereof The invention relates to the technical fields of medicinal preparations and preparation methods thereof and particularly discloses a formula of povidone iodine ointment of full water-soluble matrix and a preparation method thereof. The povidone iodine ointment consists of the following components in percentage by weight: 10 percent of povidone iodine, 0.1 to 0.5 percent of potassium iodate, 20 to 31 percent of polyethylene glycol-400, 20 to 30 percent of polyethylene glycol-4000, 5 to 15 percent of xylitol or sorbitol serving as a matrix protecting agent, 15 to 20 percent of glycerol, 0.5 to 2.0 percent of sodium dodecyl sulfate, and 7.5 to 15 percent of purified water. By using unique protective methods and means, the technical problem of low stability in preparation and storage processes of the ointment after the povidone iodine and the water-soluble polyethylene glycol matrix are mixed is solved, the povidone iodine ointment with good performance advantages is prepared, the manufacturing time is greatly shortened, the working efficiency is improved, and the povidone iodine ointment is suitable for large-scale production.
WO2013156850A1 Systems and methods for treating an opioid-induced adverse pharmacodynamic response Disclosed in certain embodiments is a method of treating or preventing an opioid-induced adverse pharmacodynamic response comprising administering to a patient in need thereof an effective amount of buprenorphine.
CN102552316A Nose washing agent and preparation method thereof The invention provides a nose washing agent and a preparation method thereof. The nose washing agent treats sea salt and sodium bicarbonate as main bulk drugs. Compared with nose washing agents prepared with the prior art, the nose washing agent of the invention has the advantages of superior sterilization effect, effective elimination of pathogenic bacteria in the nasal cavity, mildness and no stimulation, and realization of comfortableness of patients while in use.
WO2011070299A1 Tri-substituted 9h-beta-carboline (or 9h-pyrido[3,4-b]indole) derivatives, preparation of same and therapeutic use thereof The invention relates to products of the general formula (I): as well as to the isomers and salts of said products of formula (I) and to the therapeutic use thereof for treating cancer.
CN101961332A Nimodipine ophthalmic preparation and preparation method thereof The invention relates to a drug effective ingredient, in particular to a nimodipine (NMD) ophthalmic preparation and a preparation method thereof. The nimodipine ophthalmic preparation comprises a medicinal auxiliary and an effective quantity of nimodipine ingredient used for protecting optic nerves and dispersed to the auxiliary. In the embodiment of the invention, the NMD ophthalmic preparation comprises a 0.09% NMD eye drop and a 0.3% NMD eye ointment. The preparation method of the 0.09% NMD eye drop comprises the following steps of: adding 0.9 g of NMD and 0.3 g of ethylparaben into 50 ml of tween-80, and uniformly stirring, adding 600 ml of double buffer solution, heating to dissolve, adding the double buffer solution to 1000 ml, and adjusting the pH value to 6.7-7.2; filtering, sterilizing by flowing stream, and canning. The preparation method of the 0.3% NMD eye ointment comprises the following steps of: placing 3g of nimodipine in a sterilizing mortar in sterile operation, adding 5 ml of sterilized liquid paraffin, grinding into a fine paste, adding into 0.3g of ethylparaben and 50 ml of tween-80, uniformly stirring, adding an eye ointment matrix several times, uniformly grinding while adding till being 1000g, and subpackaging in a sterile way. The nimodipine ophthalmic preparation has the advantages of high efficiency, small side effect and convenient medication, and has good application prospect in the prevention and treatment of eye diseases, especially the protection of glaucoma optic nerves.
WO2011058443A1 Method and device to induce collagen biomineralisation A method of inducing the mineralization of tissue includes releasing phosphate ions adjacent to the tissue, maintaining a concentration of phosphate ions for a sufficient time to mineralize the tissue. A method to inducing mineralization of a tissue at a defined locus includes placing an implantable delivery vehicle adjacent to the defined locus, releasing phosphate ion into a fluid medium surrounding the defined locus and forming a deposit of calcium phosphate at the defined locus of the tissue adjacent to the implant surface. The tissue may be collagen, cartilage, ligament tendon, intervertebral disc or a fracture nonunion. Further, the tissue may be rendered osteoconductive and less compliant as a result of the formation of the calcium phosphate deposit at the treatment site.
WO2006103345A1 Tyrosinase inhibitors and their use for treating hyperpigmentary disorders The invention concerns the novel use for preparing pharmaceutical compositions for human or veterinary medicinal use, of compounds of general formula (I).
CA2339934C Medicine for multiple sclerosis A medicine for treatment of multiple sclerosis comprising, as an effective component, ibudilast represented by the chemical formula (1) below. Ibudilast is effective to experimental autoimmune encephalomyelitis by oral administration, and is effective to multiple sclerosis which is a disease of a central nervous system.
US7812159 Processes for preparing aromatic ethers The present invention relates to processes for preparing aromatic ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.
CN101306134A Compound Nanxing pain paste and cataplasm combination and its preparation method The invention provides Nanxing Compound Pain Paste Cataplasma Combination, which is prepared from the following by the following weight parts: 267 grams of raw arisaema tuber, 200 grams of radix aconiti, 167 grams of cloven, 167 grams of cinnamon, 300 grams of angelica, 1250 grams of asarum, 200 grams of hemlock parsley, 125 grams of panicled swallowwort root, 83 grams of frankincense, 83 grams of myrrh, and 63 grams of borneol. The auxiliary materials used for preparing Nanxing Compound Pain Paste Cataplasma Combination are as follows by the following weight parts: 1.5kg of Np-700, 60 grams of dihydroxyaluminium aminoacetate, 60 grams of tartaric acid, 15 grams of EDTA, 6kg of glycerol, 362 grams of crosslinking polyvingypyrrolidone, 11kg of purified water, 100 grams of gelatin, 100 grams of azone, 200 grams of propylene glycol, 160 grams of methyl salicylate. By adopting the materials, 1000 pieces of cataplasma herb paste are prepared. The camphor and the borneol are in powder shape. Other medicaments ethanol extracts. The invention further provides a method used for preparing the combination. Nanxing Compound Pain Paste Cataplasma Combination carries large dosage, conserves water, preserves moisture, has excellent air permeability and skin permeability, can be removed and attached repetitively without such side effects as irritability and so on.
CN1730097A Pharmaceutical composition for preventing and curing endometritis and retained afterbirth disease of milk cow The invention discloses a combined medicinal composition for the prevention and treatment of cow's endometritis, the preparation process and use, wherein the medicinal composition comprises right amount of Povidone iodine, potassium iodate, propylene glycol or glycerin, oxytocin, estrogen, carbomer, sodium hydroxide and water.
CN102793632A Component for external use The invention provides a component for external use. The component takes pyrroloquinoline quinine or medicinal salt and peptide of pyrroloquinoline quinine as an active constituent. The component can effectively improve the rough skin, eliminate wrinkles, adjust skin texture, minimize pores, and maintain the moisture.
WO2009144395A1 Polysubstituted derivatives of 2-heteroaryl-6-phenyl-imidazo[l,2- α] pyridines, and preparation and therapeutic use thereof Compounds of Formula (I): (I) wherein R1 is a heteroaryl or heterocyclic group, optionally substituted for one or a plurality of atoms or groups; X is 1 to 4 substituents, identical to or different from each other and selected from hydrogen, halogen, (C1-C10)alkyl, halo(C1-C10)alkyl, (C1-C10)alcoxy, NRaRb, nitro, or cyano, the (C1-C10)alkyl group capable of being optionally substituted for one or a plurality of groups selected from halogen, (C1-C10)alcoxy, (C1-C10)halogenoalcoxy, NRaRb, or hydroxyl; R, in positions 3, 5, 7, or 8 of Fimidazo[1,2-α]pyridine, is 1 to 4 substituents, identical to or different from each other and selected from hydrogen, halogen, (C1-C10)alkyl, halo(C1-C10)alkyl, or (C1-C10)alcoxy; R2 and R3, independently of each other, represent a hydrogen atom or a (C1-C10)alkyl group optionally substituted for an Rf group, or an optionally substituted aryl group; R4 is a hydrogen atom, a (C1-C10)alkyl group optionally substituted for an Rf group, or an aryl group optionally substituted as a base or salt having an acid added. The invention is used in therapy and in synthesis methods.
CN101006976A Anticancer medicinal composition of loaded taxane and its synergist Disclosed is a slow release injection agent of anticancer composition containing taxone and synergistic agent, which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the anticancer active constituents include taxone and/or taxone synergistic agent selected from anticancer antibiotics and/or tetrazine medicaments, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer of polyphosphate ester with polylactic acid, Polifeprosan, di-aliphatic acid and sebacylic acid, copolymer or blend of poly(erucic aciddipolymer-sebacylic acid) or poly(fumaric acid-sebacylic acid). The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 40 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.
CN102234336A Fucoidan-galactosan sulfate, extracting, separating, and purifying method thereof, and application thereof The invention discloses a fucoidan-galactosan sulfate with a novel structure. Fucoidan-galactosan sulfate provided by the present invention is a sulfated polysaccharide composed of fucose and galactose. According to the chemical constitution of the sugar chain, a fundamental chain is formed by -4-alpha-L-Fuc-(1,3)-alpha-L-Fuc-(1,3)-alpha-L-Fuc-(1,3)-alpha-L-Fuc-(1-residue. Every 4 sugar residues comprise a branched chain, which is composed of alpha-L-Fuc(1- or beta-D-Gla-(1,6)-beta-D-Gla-(1-. Sulfated group is connected to the 2 or 4 site of fucose, or on the 3 or 4 site of galactose. Meanwhile, the invention discloses a preparation method and an application of fucoidan-galactosan sulfate. Fucoidan-galactosan sulfate provided by the present invention can be exploited into medicines for treating kidney diseases.
WO2011020030A3 Methods and compositions to prevent addiction Disclosed herein is a method of reducing or preventing the development of aversion to a CNS stimulant in a subject comprising, administering a therapeutic amount of the neurological stimulant and administering an antagonist of the kappa opioid receptor, to thereby reduce or prevent the development of aversion to the CNS stimulant in the subject. Also disclosed is a method of reducing or preventing the development of addiction to a CNS stimulant in a subject, comprising, administering the CNS stimulant and administering a mu opioid receptor antagonist to thereby reduce or prevent the development of addiction to the CNS stimulant in the subject. Also disclosed are pharmaceutical compositions comprising a central nervous system stimulant and an opioid receptor antagonist. Examples of central nervous system stimulants (such as methylphenidate) and opioid receptor antagonists (such as naltrexone) are provided.
WO2010030360A1 3H-IMIDAZO[4,5-b]PYRIDIN-5-OL DERIVATIVES USEFUL IN THE TREATMENT OF GPR81 RECEPTOR DISORDERS The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.
US20120022080 Plasminogen Activator Inhibitor-1 Inhibitor The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.
CN101189960B Method for breeding selenium-rich livestock and fowls The invention discloses a method of raising livestock and poultry with rich selenium: 1-5 days before butchered, the livestock and poultry is fed with medicine continuously once or a plurality of times per day by a daily feeding dosage of 0.4mg/kg.b.w.-32mg/kg.b.w.; the medicine that the livestock or poultry is fed with is a preparation with selenium; the preparation with selenium is selenite, selenate, selenomethionine, selenium-enriched yeast, selenizing polysaccharides, selenium-enriched mushroom powder or selenium-enriched albumen powder. The medicine feeding method is that the preparation with selenium is mixed with foodstuff and/or drinking water and is taken by the livestock and poultry. The livestock and poultry raised by the method have selenium content of 20Mug/100g to 150Mug/100g in meat and of 300Mug/100g to 900Mug/100g in internal organs.
US7034044 NMDA (N-methyl-D- aspartate)-receptor subtype blockers and are used in the treatment or prevention of CNS disorders i.e. Alzheimer's, Parkinson's, etc. The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.
US7297691 Administering galanthamine and nicotinic receptors The present invention is concerned with treatment of sleep disorders by administering a cholinesterase inhibitor, and in particular, by administering galantamine or a pharmaceutically acceptable salt thereof. Also in particular, cholinesterase inhibitors that are active at nicotinic receptors and that are selective for acetylcholinesterase over butylcholinesterase are used in treating sleep disorders.
WO2006129158B1 3 - indazolyl - isoxazoline derivatives as inhibitors of phosphodiesterase type - i The present invention relates to isoxazoline derivatives, of formula (I a) which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in treating AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis or other inflammatory diseases especially in humans. Processes for preparing compounds described herein are provided, as well as pharmaceutical compositions comprising compounds described herein, and their use as phosphodiesterase (PDE) type IV inhibitors.
CN102716075A Ceftizoxime sodium-containing pharmaceutical composition The invention relates to a novel pharmaceutical preparation composition, in particular to a ceftizoxime sodium-containing preparation for injection and a preparation method for the ceftizoxime sodium-containing preparation. The ceftizoxime sodium-containing preparation for injection comprises the following components: ceftizoxime sodium, mannitol, EDTA (Ethylene Diamine Tetraacetic Acid) calcium,vitamin C, sodium hydrogen citrate, 2000ml of trisodium citrate buffer solution and water for injection.
CN1730075A Preparation method of blood enriching tablet The invention provides a Weixuekang tablet, which is a tablet form medicinal preparation prepared from crude drugs according the prescription. The tablet can be used for treating sallow complexion, megrims, syrigmus, soreness and weakness of the loins and knees.
US20050070579 Performing crystallization by using an organic solvent selected from a ketone solvent, a nitrile solvent, and a mixture thereof, or a mixture of organic solvent and water; acetone or acetonitrile can be preferably used as the organic solvent A crystal of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxytax-11-en-13-yl (2R,3S)-3-(tert-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate, which has characteristic peaks at diffraction angles (2θ) of 6.2°, 10.3°, 10.7°, 11.4°, and 12.0° in a powder X-ray diffraction pattern, and a method for preparing the aforementioned crystal, which comprises the step of performing crystallization by using an organic solvent selected from the group consisting of a ketone type solvent, a nitrile type solvent, and a mixture thereof, or a mixture of said organic solvent and water.
WO2010119942A1 Levocabastine suspension type eye lotion A composition based on an improvement on suspension type eye lotions containing levocabastine or a salt thereof as an active ingredient. A suspension type eye lotion which contains (a) 0.01-0.1% (w/v) levocabastine or salt thereof, (b) 0.0005-0.01% (w/v) benzalkonium chloride, (c) 0.00001-2% (w/v) water-soluble polymer, and (d) 0.1-5% (w/v) isotonizing agent that is at least one compound selected from sodium chloride, potassium chloride, calcium chloride, magnesium chloride, glycerol, propylene glycol, polyethylene glycol, trehalose, sucrose, sorbitol, and mannitol and which has an osmotic-pressure ratio of 0.5-2.0 has a lower antiseptic content than existing levocabastine suspension type eye lotions and, despite this, is equal to the existing levocabastine suspension type eye lotions in antiseptic efficacy. In addition, the suspension type eye lotion is superior to the existing levocabastine suspension type eye lotions in redispersibility.
CN101045715A Heterocycle inhibitor for glycogen synthase kinase gsk-3 Compounds of formula (I) where A, E, G, X, Y, and the bond --- take various meanings are of use in the preparation of a pharmaceutical formulation, for example in the treatment of a disease in which GSK-3 is involved, including Alzheimer's disease or the non-dependent insulin diabetes mellitus, or hyperproliferative disease such as cancer, displasias or metaplasias of tissue, psoriasis, arterosclerosis or restenosis.
WO2014070774A1 Methods of generating beta-lactamase resistant carbapenem compounds The present invention includes compositions, methods of making and using novel carbapenem compounds including active agents, compounds, antibacterial agents, pharmaceutically acceptable salts of C1α-C1β di-substituted carbapenem compounds, C5α substituted carbapenem compounds, C6α-C6β di-substituted carbapenem compounds and combinations thereof.
WO2008020243A1 Treatment of dna viral infections of the eye A composition for the treatment of DNA viral infections, the composition comprises a diuretic and/or a cardiac glycoside and a source of potassium ions.
US20050020638 Method of stabilizing lansoprazole The present invention provides a stable 2-(2-pyridylmethyl) sulfinyl-1H-benzimidazole (lansoprazole) and a method for stabilizing lansoprazole by use of a weakly basic material. The present invention also provides a method for the preparation of a stable lansoprazole.
CN102558185A Pyrido-pyrrole triazine compound, and preparation method and application thereof The invention relates to a novel dual inhibitor of phosphatidylinositol-3 kinase and rapamycin target protein, a preparation method and application of the dual inhibitor, in particular to a pyrido-pyrrole triazine compound with a structure shown in general formula I. a preparation method of the compound and application of the compound as a dual inhibitor of phosphatidylinositol-3 kinase and rapamycin target protein in preparation medicines for treating phosphatidylinositol-3 kinase related diseases such as tumors.
CN1887317B Externally applied liniment for treating rheumatic and rheumatoid arthritis and its preparation The externally applied liniment for treating rheumatoid arthritis consists of active components and carrier. The active components consists of frankincense 23.6-33.6 wt%, papaya 9.2-19.2 wt%, buck grass 9.2-19.2 wt%, camphor 37.7-47.7 wt% and musk 0.25-0.35 wt%; and the carrier is 70-75 % concentration alcohol solution. The preparation process includes decocting frankincense, papaya and grass, filtering to eliminate dregs, concentrating, adding ground musk and camphor and 70-75 % concentration alcohol solution, and mixing. The externally applied liniment is applied to the affected part to treat rheumatoid arthritis, joint strain sequela and other diseases.
CN101209259A Use of hyaluronic acid for chondrocyte oxidation resistance and hyperplasia The invention relates to a usage of hyaluronic acid used for improving the oxidative damage of cartilage cells, so as to promote the proliferation of cartilage cells. More particularly, the invention relates to a usage of hyaluronic acid with the molecular weight of 0.6 to 1.2 million daltons used for protecting the activate oxygen damaged cartilage cells and promoting the proliferation of cartilage cells. The invention also relates to a usage of hyaluronic acid used for producing the pharmaceutical products for the treatment or prevention of arthritis and supplying the oral foods or drinks for the improvement of arthritis symptoms.
US20110217279 Use of human biliverdin reductase and fragments thereof for the treatment of protein kinase c-delta and erk related conditions The present invention is directed to methods of modulating PKC-δ activity and PKC-δ/ERK complex activity in cells via biliverdin reductase. Methods and compositions for diagnosing and treating a PKC-δ and PKC-δ/ERK complex related condition are also disclosed.
CN1861089A Prepn. of chlorofarabin and its prepn. method A medicine clofarabine in the form of injection, powder injection, tablet, capsule etc for treating the intractable and recurrent lymphatic leukemia, acute myeloid leukemia and other abnormal myeloproliferative diseases contains clofarabine, pharmacologically acceptable carrier and/or excipient.
CN101708308A Anti-tumor medicinal composition without stimulation to gastrointestinal mucosae The invention discloses an anti-tumor medicinal composition without stimulation to gastrointestinal mucosae. The medicinal composition is prepared from the following materials in part by weight: 0.01 to 2 parts of norcantharidin, 30 to 100 parts of ginseng, 180 to 500 parts of astragalus, 180 to 500 parts of manyprickle acanto-panax root, 50 to 180 parts of common burreed rhizome, 180 to 600 parts of barbed skullcap herb, 5 to 50 parts of zedoary, 60 to 200 parts of common macrocarpium fruit, 80 to 300 parts of glossy privet fruit, 1 to 5 parts of bear gall bladder powder, 30 to 100 parts of licorice and auxiliary materials. Compared with the prior art, the medicinal composition has the efficacies of removing blood stasis, eliminating mass and eliminating toxic phagedena, and has the same curative effect as that of the conventional compound blister beetle preparation on the diseases such as primary liver cancer, lung cancer, colorectal cancer, malignant lymphoma, gynecological malignant tumors and the like; and simultaneously the medicinal composition effectively overcomes the defect that the conventional compound blister beetle preparation is stimulating to the gastrointestinal mucosae, and improves the safety of the medicinal composition.
CA2667510A1 Methods for treating disruptive behavior disorders The present invention is a method for the treatment of Disruptive Behavior Disorders including both Conduct Disorder and Oppositional Defiant Disorder comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and/or Formula 2 as herein defined and shown below. Formula 1 Formula 2 The present invention is directed to a method for the treatment of Disruptive Behavior Disorders including both Conduct Disorder and Oppositional Defiant Disorder, which includes mono-therapy and alternatively, co-therapy with at least one additional psychoactive medication.
CN102688241A Tamper resistant oral pharmaceutical dosage forms comprising opioid analgesic The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.
CN101077343A Dexibuprofen granule and preparation method thereof The present invention discloses one kind of dextro brufen granule and its preparation process, and features that the dextro brufen granule contains dextro brufen 1 weight portions, alkaline cosolvent 0-100 weight portions, stuffing 0.1-100 weight portions, adhesive 0.1-12 weight portions, corrective 0.01-0.5 weight portion, and lubricant 0.1-2 weight portions. Its preparation process includes the steps of mixing, pelletizing and packing. The effervescent dextro brufen tablet is superior to traditional orally taken dextro brufen preparation, can dissolve in water to form tasty solution, and has easy taking, high bioavailability, fast acting and other advantages.
WO2014006529A3 Compositions and methods for the treatment of moderate to severe pain The invention relates to the compounds of formula 1 or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof The pharmaceutical compositions comprising art effective amount of compounds of formula Ϊ; and methods for treating or preventing moderate to severe pain, may he formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenieral adminisiration, syrup, or injection. Such compositions may be used to treatment of muscle pain, spasticity, neuropathic pain, fibromyalgia, postoperative pain,.muscle spasticity, headache, chronic pain, sub-chronic pain and local pain.
CN1857240A Application of hypericin in preparing RNA virus resisting medicine The present invention discloses new use of hypericin. The experiment of the present inventor proves that hypericin possesses high effect of inhibiting and deactivating RNA virus, especially bird flu virus, foot-and-mouth disease virus and canine distemper virus and may be used as the active component for RNA virus resisting medicine. The RNA virus resisting medicine may be used in preventing and treating diseases caused by bird flu virus, foot-and-mouth disease virus, canine distemper virus and other RNA virus. The present invention makes hypericin possess wide application in medical science and biomedicine preparing fields.
WO2007026771A1 Injection for intravenous drip A high-content injection for intravenous drip which is prepared by adding an acidic pH regulator to an aqueous suspension containing 4-(N-(4-morpholin-4-yl)butyl)carbamoylmethyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one (Compound A) and dissolving it therein followed by, if necessary, adjusting the pH value by using a basic pH regulator. Because of being stable to light and heat, this injection is a highly useful preparation. It is preferable to adjust the pH value of the injection to 3 to 7. The concentration of the compound A is preferably from 50 mg/mL to 300 mg/mL and the viscosity of the injection is preferably from 1 mPa.s to 4 mPa.s.
CN102875477A Phenyl piperazinepyridazinone and preparation method as well as application thereof The invention relates to phenyl piperazinepyridazinone, wherein a chemical structural formula of the phenyl piperazinepyridazinone is shown as a formula (I); and in the formula (I), n is 2, 3, 4, 5 or 6, and R1 is 2-(2-methoxyl phenoxyl) ethyl group, 2-(2-methoxyl phenyl) ethyl group, 2-(4-methoxyl phenyl) ethyl group or 2-(3, 4-dimethoxyl phenyl) ethyl group. A synthesis method of the phenyl piperazinepyridazinone comprises the following step of: reacting 1-(omega-bromoalkyl)-4-(2-methoxyl phenyl) piperazine and 4-chloro-5-amino pyridazinone to obtain the phenyl piperazinepyridazinone; or reacting 2-methoxyl phenyl piperazine and 2-(omega-bromoalkyl)-4-chloro-5-amino-2H-pyridazinone to obtain the phenyl piperazinepyridazinone. The phenyl piperazinepyridazinone has an antagonistic effect on alpha 1-adrenoceptor and can be used for preparing an alpha 1-AR antagonist.
US20060189673 Phenylazole compound, production process therefor and antioxidant The present invention relates to a compound represented by formula (1): (wherein R represents a hydrogen atom or a C1-6 alkyl group which may be substituted, A represents an imidazolyl group or a pyrazolyl group, B represents a group represented by the following formula: (wherein R5 and R6 each independently represents a hydrogen atom, a cyano group, a hydroxyl group, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, or the like, k represents 0 or an integer of 1 to 15, and R5 and R6 may be identical or different from each other, when k is 2 or more), and Z represents a substituted chroman-2-yl group, a substituted 2,3-dihydrobenzofuran-2-yl, a substituted thiochroman-2-yl group, a substituted 2,3-dihydrobenzothiophene-2-yl group, or a substituted 1,3-benzoxathiol-2-yl group).
CN101066252A Aminoglucose calcium tablet and its prepn process The present invention is dispersed aminoglucose calcium tablet for preventing and treating osteoarthritis and osteoporosis and its preparation process. The dispersed aminoglucose calcium tablet has prepared with aminoglucose and calcium citrate as effective components, and excipient, disintegrant, lubricant, adhesive and wetting agent as supplementary material. Its preparation process includes crushing the materials, sieving, mixing, pelletizing and tabletting. Compared with common tablet, the dispersed aminoglucose calcium tablet has high dispersivity, high leaching speed, fast acting and other advantages.
CN103130798A Novel crystal of tiotropium bromide The invention relates to a novel crystal of tiotropium bromide, and particularly relates to tiotropium bromide crystallization, a method of preparing the crystal, crystallization composition containing the crystal, medicine composition containing the crystal, and usages of the novel crystal of the tiotropium bromide in the field of medicine. The crystal of the tiotropium bromide can meet rigorous conditions for preparing inhalation, and has the physical property suitable for inhalation and industrial production. A value d of the crystal face distance of an X-ray diffraction (XRD) spectrum of the crystal is used for representing that diffraction peaks exist.
US20080193544 Taste Masked Dosage Form Containing Roflumilast Taste masked dosage forms for oral administration of roflumilast are described.
CN102670587A Application of 7-methoxy-8-isopentenycoumarin in medicine The invention discloses application of 7-methoxy-8-isopentenycoumarin in medicine, and belongs to the field of research and development of new drugs. The immune balance of the body is regulated by an immune system through different cytokines such as TNF-alpha (tumor necrosis factor-alpha), IL-4 (interleukin-4), INF-gamma (interferon-gamma) secreted by various immune cells. If immune cytokines in vivo are in disorder, too high or too low content of immune cytokines can lead to diseases. By establishing a TNF-alpha-luc (tumor necrosis factor-alpha-luciferase) transgene, a mouse drug screening model is reported, and the situation that 7-methoxy-8-isopentenycoumarin can better inhibit the secretion of TNF-alpha are found by screening. TNF-alpha is a proinflammatory cytokine, and the abnormally high expression of the TNF-alpha can lead to autoimmune diseases such as rheumatoid arthritis and psoriasis. Based on a regulatory mechanism of an immune system, the small-molecule drug can inhibit the expression of the TNF-alpha, and thus is expected to be developed into an anti-inflammatory drug used for the treatment of inflammatory diseases.
WO2009033651A1 Titration package for neramexane and its use in the treatment of an inner ear disorder The present invention relates to a titration scheme for the administration of a 1-amino-alkylcyclohexane derivative which allows for quick attainment of an effective dose of a 1-amino-alkylcyclohexane derivative while minimizing side effects. The present invention further relates to a titration package for providing a 1-amino-alkylcyclohexane derivative (e.g., neramexane or a pharmaceutically acceptable salt thereof) in at least two different dosages. The present titration scheme/titration package may be useful in the treatment of various diseases, including tinnitus.
WO2010060030A1 Tlr ligand-nucleic acid nanostructure as a novel immune modulatory agent and method of using the same The present invention provides a composition comprising at least one TLR ligand bound to a nucleic acid nanostructure and methods of use thereof. The methods of making the composition comprising a TLR ligand bound to a nucleic acid nanostructure are also provided.
WO2009120874A2 INHIBITORS OF ANTIGEN RECEPTOR-INDUCED NF-кB ACTIVATION A method to identify selective inhibitors of antigen receptor-mediated NF-кB activation is provided, as well as compositions having one or more of those inhibitors and methods of using those inhibitors.
CN101862326A Medicine compound containing febuxostat The invention discloses a medicine compound containing febuxostat; and containing the febuxostat and surfactant, the medicine compound can be stably and quickly dissolved out and is applicable to arthrolithiasis curing.
US7345062 Substituted acylhydroxamic acids and method of reducing TNFαlevels Imido and amido substituted acylhydroxamidic acids which reduce the levels of TNFα and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propandylamino)propanoate.
CN101757112A Fig-American ginseng buccal tablet The invention relates to the field of health food, in particular to a fig-American ginseng buccal tablet, which comprises fig powder, American ginseng powder, dextrine, mannite, glucose syrup powder, lyophilized honey powder and magnesium stearate, and is characterized by comprising 3.0-4.0 parts of fig powder, 15-25 parts of dextrine, 25-35 parts of mannite, 8-10 parts of glucose syrup powder, 1.0-2.0 parts of lyophilized honey powder, 1.5-2.0 parts of American ginseng powder, and 10 percent of magnesium stearate of the total content. The invention can be added with a small amount of essence so that the taste is mellow, can be also added with a small amount of coloring matter so as to stimulate the appetite, and has the advantages of rich nutriments, antifatigue, obviously improving the immunity of the organism, good health care effect and the like.
WO2006128791A1 New derivatives of pyrrolyltriazine together with methods for obtaining them and their use as protecting agents against uv radiation The present invention relates to new pyrrolyltriazine derivatives of general formula (I) together with method for obtaining them. The physico-chemical properties of said compounds allow them to be used as absorbents of UV radiation.
CN102198134A Use of new stable Ulifloxacin hydrochloride in preparation of anti-infection medicine Ulifloxacin has low water solubility and low bioavailability. The invention relates to an Ulifloxacin salt, a preparation thereof, a kit having the medicinal antibiotic preparation and the use of the new Ulifloxacin salt in the preparation of an anti-bacterial-infection medicine. The invention particularly relates to a new medicinal preparation which is used for injection and can be stored stablyand the chemical name of which is 6-fluoro-1-methy-7-(1-piperazinyl)-4-oxo-4H-[1,3]thiazeto[3,2-alpha]quinoline-3-carboxylate. In the invention, the medicinal preparation is administrated by direct injection in form of thiabutyldine quinoline carboxylate, the solubility is improved, the bioavailability is improved and treatment effect is enhanced.
CN103263394A Cetirizine hydrochloride tablet and related substance quality control method thereof The invention aims at providing a cetirizine hydrochloride tablet and a related substance quality control method thereof which are used for overcoming the shortcomings of thermal instability, low compatibility between raw and auxiliary materials, easy yellowing in a placing process and the like of cetirizine hydrochloride. The cetirizine hydrochloride tablet is prepared by the following steps of: mixing polyethylene glycol 4000, titanium dioxide, cetirizine hydrochloride and low-substituted hydroxypropyl cellulose; wrapping the cetirizine and low-substituted hydroxypropyl cellulose by dry granulation so as to avoid the influence of heat, light and other auxiliary materials and avoid influence on the dissolution; and mixing the prepared granules and other auxiliary materials, and directly tabletting, wherein the technological flow is shortened, energy consumption and material consumption are reduced, and the yield of the cetirizine hydrochloride tablet is improved. Meanwhile, the related substances of the cetirizine hydrochloride tablet are checked by a high performance liquid chromatography, and a standard limit is set so as to control the quality better and improve the curative effect and safety.
US20090075914 Deuterium-enriched odiparcil The present application describes deuterium-enriched odiparcil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2008105384A1 Citrulline-containing tablet It is demanded to develop a tablet which can exert various useful functions of arginine and other ingredients contained therein in a living body and which is excellent in tablettability and storage stability. Disclosed is a tablet comprising citrulline or a salt thereof and other active ingredient, wherein the other active ingredient is at least one component selected from the group consisting of an amino acid (other than citrulline) or a salt thereof, an organic acid or a salt thereof and an animal/plant powder.
US8217168 Azabicyclo [3. 1. 0] hexyl derivatives as modulators of dopamine D3 receptors The present invention relates to novel compounds of formula (I) or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; p is an integer ranging from 0 to 5; R1 is halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R6; and when p is an integer ranging from 2 to 5, each R1 may be the same or different; R2 is hydrogen or C1-4alkyl; n is 3, 4, 5 or 6; R6 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such R6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR′R″; or R4 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; R7 is hydrogen or C1-2alkyl; R′ is H, C1-4 alkyl or C1-4 alkanoyl; R″ is defined as R′; R′ and R″ taken together with the interconnecting nitrogen atom may form a 5-, 6-membered saturated or unsaturated heterocyclic ring; and their use in therapy, as modulators of dopamine D3 receptors.
WO2007126857A1 Diamidine inhibitors of tdp1 The instant invention is directed towards compounds, including diamidines, that inhibit Tdpl and are useful in the treatment and/or prevention of cancer and parasitic disease.
WO2012098143A1 Use of inhibitors of atp-sensitive potassium channels for the treatment of hearing loss The present invention relates to the use of inhibitors of ATP-sensitive potassium channels for the protective (including preventive) therapy or the reduced progression of hearing loss, in particular age-related hearing loss (presbycusis) and/or noise-induced hearing loss (NIHL). Preferred is the systemic or local administration of clinically established sulfonylureas, such as, for example, glibenclamide.
US20090192170 N-((S)-1-cyclopentyl-2-oxo-2-((3aS,6aR)-3-oxodihydro-2H-furo[3,2-b]pyrrol-4(5H,6H,6aH)-yl)ethyl)-4-(4-methylpiperazin-1-yl)benzamide; osteoporosis, Paget's disease, Chagas's, malaria, gingival diseases, hypercalcemia, metabolic bone disease, bone cancer and associated pain The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof (I), wherein: R3 is cyclopentyl or cyclohexyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
WO2013087806A1 Piperazine derivatives and their use as positive allosteric modulators of mglu5 receptors This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
WO2013048158A3 Novel usage for eupatilin The present invention provides a medicinal and/or a food usage of eupatilin for treating, improving, and/or preventing at least one condition selected from bone disease, menopausal disorder, cardiovascular disease, neurodegenerative disease, or obesity. Advantages of the present invention includes little or no possibility of side effects such as cancer, and effective treatment, improvement, and/or prevention of the at least one condition selected from bone disease, menopausal disorder, cardiovascular disease, neurodegenerative disease, and obesity.
US20080171784 Stabilization of the pharmaceutical active solid substance atorvastatin (Lipitor) alone or in a mixture with other solid substances embedded in a surrounding gaseous mixturewhere a partial pressure of oxygen of at < 2 kPa is maintained; amorphous; blister-pack using an oxygen self-activating absorber Stabilization of the pharmaceutical active solid substance atorvastatin alone or in a mixture with other solid substances embedded in a gaseous mixture is carried out in such a manner that in the surrounding gaseous mixture a partial pressure of oxygen of at most 2 kPa, preferably less than 1 kPa, more preferably less than 0.4 kPa is maintained. The corresponding partial pressure is achieved either by use of oxygen absorbers, by packaging under a pressure of 0.3-10 kPa, or by packaging under a slight overpressure of an inert gas, preferably nitrogen, the gas being introduced, by means of nozzles, into the cavities, optionally also into the space of the press roller and of the wiper station.
CA2671528A1 Use of fluocinolone acetonide,tretinion and hydroquinone cream in melasma maintenance therapy The present invention provides for a method of using triple combination of fluocinolone acetonide, hydroquinone and tretinoin for the maintenance therapy of melasma to prevent hype rpigmentat ion recurrence or reduce the severity of the hyperpigmentation recurrence.
WO2012149557A1 miR-33 INHIBITORS AND USES THEREOF TO DECREASE INFLAMMATION The inhibition of miRNA miR-33 is shown to promote the polarization of macrophages from an Ml to an M2 phenotype. MiR-33 inhibitors are therefore useful for treating inflammation in subjects. Endogenous microRNAs can be silenced using antagomirs. The miR-33 inhibitor is preferably an antagomir having a single - stranded nucleic acid sequence that is complementary to at least 12 contiguous nucleotides in miR-33 and therefore forms a duplex with miR-33 under physiological conditions.
WO2014005182A1 Phosphoinositide 3-kinase (pi3k) inhibitors The invention relates to compounds, and uses of the compounds, that are inhibitors of the enzyme phosphoinositide 3-kinase (PI3K). More particularly the compounds are selective inhibitors of one or more isoforms of PI3K. In particular embodiments the compounds are selective inhibitors of one isoform of PI3K.
EP2046358A1 Induction of analgesia in neuropathic pain The present invention relates to agents which are capable of inducing analgesia in chronic neuropathic pain, associated methods and uses thereof. In particular, the present invention provides compounds capable of activating the TRPM8 receptor for the treatment of chronic neuropathic pain.
EP2545919A1 Treatment of synucleinopathies Methods and compositions useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease, and Multiple System Artophy, or other neurodegenerative diseases are provided. The treatment including administering to a subject a farnesyl transferase inhibitor compound.
US7662553 Polymorphisms in the ERCC1 gene for predicting treatment outcome The invention provides compositions and methods for determining the increased risks for recurrence of certain cancers and the likelihood of successful treatment with one or both of chemotherapy and radiation therapy. The methods comprising determining the type of genomic polymorphism present in a predetermined region of the gene of interest isolated from the subject or patient. Also provided are nucleic acid probes and kits for determining a patient's cancer risk and treatment response.
WO2009093737A1 Anti-obesity pharmaceutical composition Disclosed is a pharmaceutical composition which has little adverse side effects including abdominal pain and also has an excellent subcutaneous fat- or visceral fat-diminishing effect. The pharmaceutical composition comprises the following components (A) and (B): (A) at least one herbal medicine selected from the group consisting of divaricate saposhnikovia miraculous powder (fang-feng-tong-sheng-san) and major bupleurum decoction (da-chai-hu-tang); and (B) at least one pantethine component selected from pantethine, a salt of pantethine, pantothenic acid, a salt of pantothenic acid, pantetheine and panthenol.
CA2680272A1 Droxidopa and pharmaceutical composition thereof for the treatment of fibromyalgia The present invention provides methods of treating fibromyalgia or other diseases or conditions causing widespread pain and/or fatigue. In particular, the invention provides pharmaceutical compositions comprising droxidopa alone, or in combination with one or more further active agents, that can be used in the inventive methods. The methods of treatment can comprise treating, preventing, reducing, or eliminating a variety of symptoms recognized as indicative of fibromyalgia, such as chronic pain, allodynia, hyperalgesia, fatigue, sleep disturbance, and depression.
EP2567955A2 Crystal of salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide or of solvate thereof and processes for producing these A crystal of a 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide hydrochloride, hydrobromide, p-toluenesulfonate, sulfate, methanesulfonate or ethanesulfonate, or a solvate thereof.
EP1375496B1 N-aryl-substituted cyclic amine derivative and medicine containing the same as active ingredient A compound having excellent squalene synthetase inhibitory activity. It is a compound (I) represented by the following general formula, a salt thereof, or a hydrate of either. (I) In the formula, R1 means optionally substituted vinyl or an optionally substituted aromatic ring; n is an integer of 0 to 2; X, Y, and Z are the same or different and each means optionally substituted carbon, nitrogen, etc.; CyA means an optionally substituted 5- to 14-membered nonaromatic cyclic amino group optionally containing oxygen or sulfur; W means -C=C-, etc.; and A means a group of the formula (II) (wherein R8 represents hydrogen, hydroxy, etc.; B2 represents optionally substituted carbon or nitrogen; and c is 0 or 1), etc.
CN103301129A Application of tropane compound Maraviroc in preparation of antitumor drugs The invention belongs to the field of medicines, in particular relates to an application of a tropane compound Maraviroc in preparation of antitumor drugs, and further provides an application in preparation of antitumor drugs. According to the invention, the MVC has an invasion ratio being not lower than 38% and a migration inhibition ratio being not lower than 26.7% to tumor cells, particularly to lung cancer cells.
CN1762388A Tasty, refreshing, sterilizing, yin-nourishing health care product or drug formula and preparation method thereof The invention discloses a tasty, refreshing, sterilizing, yin-nourishing health care product or drug formula and preparation method, which comprises the effective components of medicinal herbal plants including blueberry, bee glue, menthanol and various vitamins proportionally, refining and dissolving with right base, carrying out high pressure homogeneous treatment and ultramicro emulsification, melting with dissolved base at a predetermined temperature proportionally, thus obtaining various preparations.
CA2256687C Benzimidazole derivatives for treating gastrointestinal inflammatory diseases The present invention relates to benzimidazole derivatives of formula (I), in which the phenyl moiety is substituted with lower alkyl in 2- and 6-position, which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.
US20090042879 Phthalazinone derivatives and pharmaceutical compositions comprising the same The present invention provides a novel compound having an excellent PDE4 inhibitory activity and TNF-α production-suppressing activity, and also provides a preventive and therapeutic agent for atopic dermatitis or the like. The present invention includes a novel phthalazinone derivative of the following general structural formula [1] or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising it as an active ingredient. In the structural formula [1], the partial structure bridging the 6-position and the 7-position represents a single bond or a double bond; R1 and R2 are the same or different and each represents alkyl or the like; Y represents phenylene or the like; Z represents alkylene or the like; and R3 represents a mono- to tri-cyclic saturated or unsaturated cyclic amino group or the like optionally substituted with R31 and R32, wherein R31 and R32 represent alkyl or the like.
CN101040904A Drug for scald and its preparing method The invention relates to a pharmaceutical composition for treating burns and scalds and process for preparation, wherein the composition is prepared from boneol, white alum, purple perilla, cyathula root, sesame oil and bleached bees wax for medical purpose. The medicament can be applied by plastering onto the suffered positions.
CN102579375A Lipid lowering medicament orally disintegrating tablets and preparation method thereof The invention discloses lipid lowering medicament orally disintegrating tablets and a preparation method thereof, and relates to the lipid lowering medicament orally disintegrating tablets and a prescription and a process for preparing the lipid lowering medicament orally disintegrating tablets by using a freeze drying method. The lipid lowering medicament orally disintegrating tablets are prepared from a main medicine and medicinal auxiliary materials, are taken without water, can be quickly disintegrated in mouth and are suitable for dysphagia patients such as the old and children to take; meanwhile, the lipid lowering medicament orally disintegrating tablets are also suitable for cardiovascular patients who travel or go on business trips frequently to take, and have the advantages of convenience for taking, low first pass effect and low irritation to digestive tract mucosa and have board market application prospect; and the side effect of the lipid lowering medicament can be obviously reduced through the lipid lowering medicament orally disintegrating tablets provided by the invention. In addition, the invention also relates to the preparation method of the lipid lowering medicament orally disintegrating tablets.
WO2005083074A1 Tumor antigen peptides Novel peptides which are useful as tumor antigen peptides. More specifically speaking, novel HLA-A24-restricted tumor antigen peptides, a peptide vaccine using the same, a DC vaccine, an antibody and a cytotoxic T cell.
CN101028343B Total alkaloid of meadowrue corydalis and its purification and medicinal composition A meadowrue corydalis alkaloid used to prepare the medicines for preventing and treating viral hepatitis is prepared from meadowrue corydalis root through extracting, dissolving in acidic water, filtering, chromatography, eluting, concentrating and drying.
US20110124599 2,4-Pyrimidinediamine Compounds and Prodrugs and Their Uses The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I)-(III): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.
WO2006061791A3 Novel diazabicyclononene derivative The invention relates to a novel 3,9-diazabicyclo[3.3.1]nonene derivative and the enantiomers thereof and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing at least one compound of formula (I) or (I’) and especially their use as inhibitors of renin.
WO2011005871A1 Substituted 8-[6-carbonylamine-3-pyridyl]xanthines as adenosine a2b antagonists Provided herein are substituted 8- [6 -carbonylamino-3 -pyridyl] xanthines of formula (I) and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). and stereoisomers and pharmaceutically acceptable salts thereof;
CN103027921A Application of Houttuynoid B in preparation of drug for treating rheumatoid arthritis Houttuynoid B for treating immunity inflammation is used for preparing a drug for treating rheumatoid arthritis. Terfenadine and diclofenac sodium are adopted as a control; and the Houttuynoid B has a clear curative effect. The use of the Houttuynoid A related in the invention in the preparation of drug for treating rheumatoid arthritis disclosed by the invention is firstly disclosed. The framework type is a brand-new framework type and has an unexpected strong effect of restraining the bacterial activity, and so the Houttuynoid B is impossibly reveled by other compounds, and has outstanding substantial characteristics. Meanwhile, the Houttuynoid B has significant progress in preventing and treating rheumatoid arthritis.
CN102813666A Application of notoginsenoside R1 in medicine for preventing and treating neurologic and ophthalmic diseases The invention provides application of notoginsenoside R1 in preventing and treating neurologic and ophthalmic diseases, and particularly in preventing and treating retinopathy appeared in obstruction of the central retinal vein or systemic diseases. The neurologic and ophthalmic diseases comprise cerebral ischemia retinopathy, diabetic retinopathy, renal retinopathy, hypertensive retinopathy, arteriosclerotic retinopathy, hyperlipidaemia retinopathy or the like. In the invention, experiments show that obvious physiological activity exhibiting by the notoginsenoside R1 for retinopathy has an important function in preventing and treating neurologic and ophthalmic diseases, and meanwhile, the notoginsenoside R1 has wide market potential in development of relative medicines.
CN1626098A Clindamycin hydrochloride oral desintegration tablet and prepartion method An oral disintegrating tablet of antibacterial chindamycin hydrochloride is prepared from clindamycin hydrochloride, flavouring and disintegrant. Its advantage is high disintegrating speed.
EP1910350A1 2 -heterocyclyloxybenzoyl amino heterocyclyl compounds as modulators of glucokinase for the treatment of type 2 diabetes Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
WO2014078059A1 Methods for the treatment of sialorrhea The present invention provides safe and effective methods for the treatment of sialorrhea (excessive drooling) by administering an effective amount of N-desethyloxybutynin, or an optical R- or S-isomer thereof. N-desethyloxybutynin is a metabolite of oxybutynin and has higher affinity for receptors present in the parotid glands (the salivary glands in humans) than oxybutynin.
WO2006059713A1 Preventive and/or therapeutic agent for drug dependence A preventive and/or therapeutic agent for drug dependence which contains as an active ingredient either a compound having antagonistic activity against an adenosine A2A receptor, such as a xanthine derivative represented by, e.g., the formula (I) (wherein R1, R2, and R3 are the same or different and each represents hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; R4 represents cycloalkyl, -(CH2)n-R5, or the formula (II); and X1 and X2 are the same or different and each represents oxygen or sulfur) or a pharmacologically acceptable salt of the compound.
EP2391212A1 Bridged compounds as hiv integrase inhibitors Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, χ3, Y, Z, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
CN101214301A Qingkailing freeze-drying preparations and preparation thereof The present invention provides Qing Kai Ling and a preparation method thereof, made from 11 to 22 portions of choleic acid, 175 to 325 portions of Concha Margaritifera Usta, 13 to 25 portions of hyodeoxycholic acid, 87 to 163 portions of cape jasmine fruit, 87 to 163 portions of buffalo horn, 700 to 1,300 portions of radix isatidis, 17 to 33 portions of baicalin, 70 to 130 portions of honeysuckle and 7 to 13 portions of lactose. Compared with the prior technology, the lyophilized preparation provided by the present invention has the characteristics of loose texture, low water content, good stability, accurate dosage, pleasant appearance, quick effect and convenient storage, thus effectively ensuring the clinical effect of the preparation.
US20100285096 Hygiene Article Having Calcium Sugar Phosphate A hygiene article having calcium sugar phosphate is provided. The calcium sugar phosphate reduces the production of Toxic Shock Syndrome Toxin-1 (TSST-1) by Staphylococcus aureus.
US20090270423 Antibacterial small molecules and methods for their synthesis The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.
EP1191099B1 Novel polypeptide and dna thereof A novel polypeptide; a DNA encoding the same; drugs containing the polypeptide or DNA; a method of screening a compound promoting or inhibiting the activity of the above polypeptide or its salt; a screening kit therefor; the compound or its salt obtained by this screening; drugs containing the above compound or its salt and the like. The above-described polypeptide and the DNA encoding the same are usable, for example, in diagnosing, treating and preventing bone and joint diseases and pathologic anagiogenesis. The polypeptide is also useful as a reagent for screening a compound promoting or inhibiting the activity of the polypeptide or its salt.
EP2731939A1 New crystalline form The invention concerns a new polymorphic form of R-(+)-α-lipoic acid and a process for the preparation thereof, in addition to the compositions that contain it and its use as a medicine or food supplement.
CN101862324B Application of monascus color components and derivatives thereof in fighting cancers The invention provides application of monascus color components and derivatives thereof in preparing the drugs for fighting cancers, belonging to the technical field of monascus compound application. The invention solves the problem of narrower application range of the monascus color components and derivatives thereof in the prior art. The series compound comprises rubropunctamine, monascorubramine, monascin, ankaflavin, rubropunctatin, monascorubrine, monasfluore A, monasfluore B and derivatives thereof. The compound can be used as the drug and health care product additive for preventing andtreating cancers and has little toxic or side effects on normal cells of human bodies.
EP1806138A1 Anti-tumor agents comprising boroproline compounds A method for treating subjects with abnormal cell proliferation is provided. The method involves administering to subjects in need of such treatment an effective amount of an agent of Formula (I), to inhibit cell proliferation such as that associated with tumor growth and metastasis. A method for inhibiting angiogenesis in an abnormal proliferative cell mass by the administration of an agent of Formula (I) is also provided. The preferred compounds are boroproline derivatives.
CN103432108A Uses of N-3 unsaturated fatty acid in preparation of hematopoietic stem cell mobilization promoters Preliminary researches of the influences of n-3 unsaturated fatty acid to the medullary hematopoietic function show that the n-3 unsaturated fatty acid can promote the proliferation and migration of medullary hematopoietic stem cells and improve the quantities of extramedullary hematopoietic stem cells and hematopoietic precursors through adjusting the expression of a hematopoietic cell factor SDF-1alpha and a matrix metalloprotease 12 (MMP-12) in medullary hematopoietic microenvironment, and the n-3 unsaturated fatty acid can mobilize the medullary hematopoietic stem cells. Potential application values are provided for further research of biologic functions of the n-3 unsaturated fatty acid and use of the n-3 unsaturated fatty acid as a mobilization agent of the hematopoietic stem cell in hematopoietic stem cell transplantation.
WO2014154026A1 PI3K AND/OR mTOR INHIBITOR PRODRUG Provided are a compound as represented by general formula (I), pharmaceutically acceptable salt and stereoisomer thereof, and pharmaceutical composition containing the compound of general formula (I). Also provided are uses of the compound, pharmaceutically acceptable salt and stereoisomer thereof in the preparation of drugs for treating and/or preventing proliferative diseases.
CN102432599A Crystal form of oxalate of dipeptidyl peptidase inhibitor and preparation method and application thereof The invention discloses a novel crystal form of oxalate of dipeptidyl peptidase inhibitor, namely, (s)-1-(2-(2-(3-(3,4-dimethoxyphenyl)-2-oxo-1-imidazolidinyl)ethylamino)acetyl)-2-cyanpyrrolidine oxalate. In X-ray powder diffraction of the crystal form, characteristic peaks occur at 2 theta diffraction angles of 4.5+/-0.1, 5.5+/-0.1, 9.0+/-0.1, 10.9+/-0.1, 16.4+/-0.1, 17.7+/-0.1, 18.1+/-0.1, 22.0+/-0.1, 22.7+/-0.1, 25.6+/-0.1, 28.1+/-0.1, 28.4+/-0.1 and 32.0+/-0.1. The crystal form disclosed by the invention is superior to the original oxalate in stability, and is more stable for light, heat and humidity and convenient to store and transport; the cost of the DPP-IV (dipeptidyl peptidase-IV) inhibitor in transportation and preservation processes is decreased; and the safety of the product is further guaranteed.
CN102846552A Preparation and application of docetaxel lipid nanoparticle The invention discloses preparation and application of a docetaxel lipid nanoparticle. The docetaxel lipid nanoparticle mainly consists of docetaxel, a solid-state lipid material, a liquid-state lipid material, an emulsifying agent and normal saline for injection with treatment effective dose. The docetaxel lipid nanoparticle is proper in grain size, uniform in distribution and high in packaging ratio, can be stably stored, and has good biocompatibility and degradability; and moreover, the docetaxel is carried in the lipid nanoparticle, so that the targeting property and endocytosis of cancer cells can be improved, the antineoplastic curative effect is improved, and the toxic and side effects are reduced.
US20080119386 Nutritional formula for athletes' recovery A nutritional composition for athletes comprising in combination components for reducing oxidative stress, components for energy production and for maintaining lean muscle, the key component of which is SOD/gliadin.
US20120208862 Rip140 regulation of glucose transport Inhibition of RIP140 increases glucose transport. Compounds that inhibit RIP140 expression or activity are useful for treating disorders associated with aberrant glucose transport (e.g., diabetes), treating obesity, increasing metabolism (e.g., fatty acid metabolism), and increasing brown fat.
EP1390372B1 1-oxa-3,9-diaza-spiro'5,5]undecan-2-ones derivatives and its use as antagonist of the neurikinin receptor The invention relates to compounds of general formula (I) wherein (R1)n is independently from each other halogen, lower alkyl or lower alkoxy; R2 is hydrogen, lower alkyl, lower halogen-alkyl, -(CH¿2?)m-OH, -(CH2)m-NR2, -(CH2)mO-lower alkyl, -(CH2)m-C(O)-NR2, or is -(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, -(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl; R is hydrogen or lower alkyl and may be the same or different in case of R2; n is 0, 1, or 2; m is 0, 1, 2, 3 or 4; and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.
US20110269724 Combination Therapy with Non-Selective COX Inhibitors to Prevent COX-Related Gastric Injuries The present invention is directed to nicotinamide, nicotinamide derivatives and prostaglandin mimetics, alone or in combination with an NSAID, and their use in treating pain, inflammation, and/or gastrointestinal toxicty,
US20100324113 Delivery Method The present invention relates, in general, to siRNA and, in particular, to a method of effecting targeted delivery of siRNAs and to compounds suitable for use in such a method.
US6908999 Process for the preparation of {2-[4-α-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy} acetic acid and novel intermediates therefor The invention refers to a novel process for the preparation of {2-[-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy}acetic acid, which comprises hydrolyzing an N,N-disubstituted {2-[-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy}acetamide, wherein said substituents are selected from alkyl groups having 1 to 4 carbon atoms optionally substituted by a phenyl group, alkenyl groups having 2 to 4 carbon atoms or cyclohexyl groups, or the substituents together with the adjacent nitrogen atom of the acetoamido group, form a morpholino group.
EP1681922A2 Method for treating athlet s foot A method of treating a patient having a fungal infection comprises administering an effective fungal infection treatment amount of an antiviral agent, such as valacyclovir, to eliminate the symptoms of the fungal infection.
CA2332535C Antiangiogenic drug to treat cancer, arthritis and retinopathy Compounds having Formula (I) or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of inhibiting angiogenesis in a mammal.
US8222274 Pyrrole derivative or salt thereof [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
US20090118331 Use of Lobeline Epimers in the Treatment of Central Nervous System Diseases, Pathologies, and Drug Abuse Methods of delivering or administering stabilized formulations or compositions having predetermined ratios, or range of ratios, of constituent epimers to an individual or a mammal for treatment of central nervous system diseases, pathologies, and drug abuse and compositions for stabilizing the compositions. In one embodiment, the predetermined ratios of constituent epimers, or range of ratios, are predetermined ratios of 2-[6S-(2S-hydroxy-2-phenyl-ethyl)-1-methyl-piperidin-2R-yl]-1-phenyl-ethanone (2R-lobeline) and its epimer, 2-[6S-(2S-hydroxy-2-phenyl-ethyl)-1-methyl-piperidin-2S-yl]-1-phenyl-ethanone (2S-lobeline). In embodiments, the stabilized formulations or compositions of 2R- and 2S-lobeline are provided in the ranges between 1 part 2R-lobeline to 10000 parts 2S-lobeline to 10000 parts 2R-lobeline to 1 part 2S-lobeline, or in the range of a 1 to 1 mixture of 2R- and 2S-lobeline, so that the predetermined epimeric ratio of 2R- and 2S-lobeline is delivered or administered to the blood, plasma or tissues of a patient so treated.
US20110098306 Uses of tetrahydrobiopterin, sepiapterin and derivatives thereof The present invention discloses that diabetic rats showed a reduction in nitrergic relaxation of the gastric, impaired nNOS dimerization, decreased BH4 and GTPCH1 levels and thus, are more susceptible to develop diabetic gastroparesis. The use of tetrahydrobiopterin and its derivatives and sex steroid hormones as disclosed herein provides a novel strategy for therapeutic intervention of diabetic gastroparesis and any other gut-related diseases. Additionally, the present invention also discloses methods to determine risk of developing gastroparesis in an individual that are drawn to detecting variations in the activity and levels of GCH gene and in gene encoding sex steroid hormone receptor.
CN101332183A O/W emulsification preparation containing steride The invention provides a preparation with high stability for restraining separation of O/W type emulsification preparations containing steroid compound and Vaseline. The invention also provides O/W type emulsification preparations containing steroid compound, Vaseline and methyl cellulose.
WO2014135043A1 Crystal form of ixabepilone and the preparation method and use thereof Provided in the present invention is a new crystal form M of ixabepilone, which can be characterized by X-ray powder diffraction (XRD) spectrum, differential scanning calorimetry (DSC) spectrum, infrared absorption spectrum, etc. At the same time, also provided in the present invention is a preparation method and the use of the crystal form M of ixabepilone.
US6939989 Side-chain halogenated amino dicarboxylic acid derivatives as medicaments for treating cardiovascular diseases Compounds of the general formula (I) wherein R1 represents halogen, R2 represent H or halogen, and R3 represents C3-8-cycloalkyl, C3-8-cycloalkenyl, or optionally substituted phenyl, pharmaceutical compositions containing such material, and methods of using such materials in the treatment of various diseases are disclosed and claimed.
US6846832 Highly selective monoamine oxidase B inhibitors; treating Alzheimer's disease, Parkinson's disease, and senile dementia 2,3-Dihydro-isoindol-1-one derivatives, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them, for the prevention and treatment of diseases which are mediated by monoamine oxidase B.
CA2305799C Composition for the treatment of nicotine addiction containing a nicotine receptor antagonist and an anti-depressant or anti-anxiety drug The present invention encompasses methods of treating patients for tobacco addiction and nicotine addiction, for palliating the effects of nicotine withdrawal, for providing or facilitating the effects of smoking cessation therapies and as long-term smoking cessation maintenance therapy. The invention also includes related pharmaceutical compositions comprising nicotine receptor antagonists and either an anti-depressant or an anti-anxiety drug. Specific combinations of drugs (mecamylamine HC1 and bupropion HC1) as well as mecamylamine in combination with certain drug classes (e.g., anti-anxiety drugs and anti-depressants) comprise the pharmaceutical compositions disclosed. These compositions are also contemplated for use in the treatment of cocaine addiction and the treatment of alcohol dependence.
CA2344690C Fructosamine oxidase: antagonists and inhibitors Methods of reducing the consequences of macrovascular and microvascular damage in a diabetic patient reliant upon the inhibition and/or antagonism of Fructosamine oxidase in the patient. Inhibition and/or antagonism can involve the use of copper chelating agents, substrate analogues or hydrazine compounds.
WO2013126636A1 Methods for treating non- small cell lung cancer using tor kinase inhibitor combination therapy Provided herein are methods for treating or preventing advanced non-small cell lung cancer, comprising administering an effective amount of a TOR kinase inhibitor and an effective amount of erlotinib or a cytidine analog to a patient having advanced non-small cell lung cancer.
WO2008062453A3 Composition containing nicotine base aromatic oils and alkyl salicylate for the delivery of nicotine base in vapour form Composition comprising 1-99weight % nicotine base and 1-99wt% C. sub. 1-C. sub.5 alkyl salicylate (preferably methylsalicylate ) for use in the treatment of disorders of addiction and smoking in particular characterized in that nicotine base is released in vapor form.
WO2014090990A1 Leukotriene pathway antagonists for the treatment of dementia, cognitive deficits in parkinson's disease and/or learning and memory deficiencies in parkinson's disease The invention relates to a pharmaceutical composition comprising a leukotriene antagonist or a leukotriene receptor antagonist for the treatment of a subject suffering from dementia in Parkinson's disease. Further, the invention provides a pharmaceutical composition comprising a leukotriene antagonist or a leukotriene receptor antagonist for retrieval or improvement of learning processes or learning deficits and/or the prevention, retrieval or improvement of memory loss or memory impairment in a subject suffering from dementia in Parkinson's disease. The pharmaceutical composition may comprise montelukast for the treatment of subjects suffering from dementia in Parkinson's disease or for retrieval or improvement of learning processes or learning deficits and/or the prevention, retrieval or improvement of memory loss or memory impairment in a Parkinson's disease subject.
US7429666 Pyridine analogs as C5a antagonists The present invention provides novel compounds of Formula I which are antagonists of the C5a receptor. Compounds of the present invention are useful for the treatment of various C5a-mediated diseases and disorders; accordingly the present invention provides a method for the treatment of C5a-mediated diseases using the novel compounds described herein, as well as pharmaceutical compositions containing them.
CN101036763A Medicated vaginal suppository A Ê®™® for vaginal is made coil-like suppository through handing the fine cotton yarn or non-woven fabrics, high grade paper or the other material with water absorption and no stimulation, a pulling line being set on one end of suppository. The inner of the coil-like suppository absorbs the liquor manufactured by sophora flavescens ait, radix stemonae sremona, cnidium fruit, giant knotweed, shrubalthea bark and so on or nanometer silver solution or sterilization nursing medical liquor. The suppository is formed according to female physiological charateristic, so that it is easy to use, soft, elastic, comfort and nonirritative. Using the said suppository, the liquor can take sustained action on the vaginal wall to make the whole vaginal wall and posterior fornix of vagina contact the medicine, moreover the medical liquid may not poured off to contaminate the drawer.
CN101912369B Method for preparing bendamustine hydrochloride freeze-dried preparation The invention discloses a method for preparing bendamustine hydrochloride freeze-dried preparation. In the method, the bendamustine hydrochloride is dissolved in medicinal ethanol first and then mixed with water-containing solution, and the mixture is stored at low temperature, so long-time contact between the bendamustine hydrochloride and water is prevented, and the hydrolyzation speed of the bendamustine hydrochloride is reduced because of the low-temperature storage. Moreover, for improving the situation that stable freeze-dried preparation with high re-dissolubility and beautiful appearance cannot be obtained by using organic solvent ethanol in the prior art, the inventor, through deep study, finds that the stable freeze-dried preparation with high re-dissolubility and beautiful appearance can be realized by using the safe medicinal ethanol. The bendamustine hydrochloride freeze-dried preparation prepared by the method has the advantages of low impurity content, low organic solvent residue content, high stability, beautiful appearance, high re-dissolubility and applicability to clinical application and industrial production.
CN102526169A Ointment for curing psoriasis and preparation method thereof Provided are ointment for curing psoriasis and a preparation method thereof. The ointment is mainly composed of alligator oil, peanut oil, charcoal dust, vitriol and Vaseline. The weight proportion of all components of the ointment is 50 milliliters of the alligator oil, 100 milliliters of the peanut oil, 100 grams of charcoal dust sieved 100 meshes, 50 grams of vitriol ground for 100 meshes and 700 grams of Vaseline. The preparation method comprises the steps of taking alligator fat to clean up, placing the fat in an appropriate container, heating to refine, taking oil, removing residues and placing to reserve; mixing the alligator oil and the peanut oil as A, and furthermore mixing the charcoal dust with the vitriol as B; gradually adding A and B to be mixed and ground; adding the A and B in gradation mode into the Vaseline which has been melted in water bath and cooled to 40 DEG C to 60 DEG C after the A and B are fully mixed and ground, evenly grinding, and filling into bottles in splitting mode. The ointment has good effects on curing psoriasis without any side effect.
US7297779 An oligonucleotide that inhibits the function or expression of Asef (APC-stimulated guanine nucleotide exchange factor) The present invention provides an agent for inhibiting metastasis of colorectal cancer and a method for inhibiting metastasis of colorectal cancer, which inhibit the function of Asef (i.e., binding activity to the APC gene product or guanine nucleotide exchange factor activity) that binds to the gene product of the tumor suppressor gene APC that plays an important role in tumorigenesis and in developmental processes, and/or inhibit the expression of the Asef gene.
US20130028984 Natural tissue scaffolds as tissue fillers Tissue fillers derived from decellularized tissues are provided. The tissue fillers can include acellular tissue matrices that have reduced inflammatory responses when implanted in a body. Also provided are methods of making and therapeutic uses for the tissue fillers.
US20100331385 Pyrazole urea derivatives used as kinase inhibitors Compounds of Formula (I) where R1 and R2 are as defined herein, and pharmaceutically acceptable salts thereof, are useful in the treatment and prevention of various disorders mediated by kinases
CN102702126A Compound for anesthetics The invention provides an organic compound for anesthetics, functioning as sedative/hypnotic and used for anesthetization.
US20130023561 Facially Amphiphilic Polymers and Oligomers and Uses Thereof The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.
US20050020516 Effects of combined administration of farnesyl transferase inhibitors and signal transduction inhibitors The present invention relates to methods of reducing proliferation of cells, enhancing apoptosis of cells or both in an individual in need thereof, comprising administering to the individual a combination of at least one farnesyl transferase inhibitor (FTI), such as an inhibitor of Ras function, and at least one signal transduction inhibitor (STI) in a therapeutically effective amount, wherein proliferation of cells is reduced and/or apoptosis of cells is enhanced in the individual. In one embodiment, the invention relates to a method of reducing proliferation of STI resistant cells, enhancing apoptosis of STI resistant cells, or both in an individual in need thereof, comprising administering to the individual a combination of at least one FTI and at least one STI in a therapeutically effective amount, wherein proliferation of STI resistant cells is reduced and/or apoptosis of STI resistant cells is enhanced in the individual. The present invention can be used to treat leukemia (e.g., CML) in an individual comprising administering to the individual a combination of at least one FTI and at least one STI in a therapeutically effective amount.
CN103040818A Drug composition containing amoxicillin sodium and clavulanate potassium compound The invention provides a drug composition containing an amoxicillin sodium and clavulanate potassium compound. The drug composition comprises the following components in parts by weight: 6-10 parts of amoxicillin sodium, 1-2 parts of clavulanate potassium, 10-20 parts of mannitol and 1-2 parts of sodium sulfite. The pH value of the drug composition is 8.5-9.5. According to the drug composition, as amoxicillin sodium, clavulanate potassium, mannitol and sodium sulfite are compounded, and the pH value is regulated, the drug stability can be improved, and the contents of insoluble particles and relevant materials are controlled in an allowable range. In addition, with the adoption of a preparation method of the drug composition, the water content can be effectively reduced, so that the drug stability is further improved.
US20110008460 Biomimetic hydroxyapatite composite materials and methods for the preparation thereof The present invention is related to methods for preparing composite materials, which include nanoscale hydroxyapatite, and the composite materials and articles prepared therewith.
WO2006104870A3 Methods of treating benign prostatic hyperplasia or lower urinary track symptoms by using pde 5 inhibitors The use of PDE 5 inhibitors in methods for the treatment of benign prostatic hyperplasia or lower urinary tract symptoms and other physiological disorders, as a monotherapy and in combination with other active agents is disclosed. For example, a representative compound useful in the methods of the invention is: formula (I).
EP2078019A2 Purines as pkc-theta inhibitors A chemical genus of purines, which are useful as PKCϑ inhibitors, is disclosed. The genus is represented by the formula (I); A representative example is: (II)
CN103735519A Deferasirox granules and preparation method thereof The invention provides deferasirox granules and a preparation method thereof, and belongs to the field of medicinal preparations. The deferasirox granules comprise a main component and auxiliary components, wherein deferasirox serves as a main component; the auxiliary components include a filling agent, a disintegrating agent, an adhesive, a surface active agent, a corrigent, etc. The deferasirox granules can be quickly dissolved in water to form uniform suspension, taste is great, and the deferasirox granules are convenient to carry, accurate in quantifying, easy to divide in dose, and high in bioavailability, etc.; the deferasirox granules can improve patient compliance and are particularly suitable for children.
US20100063142 o/w/o EMULSION CONTAINING LIGNAN COMPOUNDS AND COMPOSITION CONTAINING THE SAME An O/W/O emulsion composition having at least one of lignan-class compounds dissolved in an internal oil phase is disclosed. This composition can be produced by a process comprising the steps of 1) dissolving at least one of lignan-class compounds in oil or fat to prepare a lignan-class compound dissolving liquid; 2) emulsifying the lignan-class compound dissolving liquid in a water phase to form an O/W emulsion; and 3) further emulsifying the O/W emulsion in an oil phase to prepare an O/W/O emulsion. This is a lignan-class compound containing composition that is enhanced in the amount of bodily absorption of lignan-class compounds.
CN102796166A Glucose-modified 4H-beta-carboline carboxylic acid derivative and preparation method and application thereof The invention discloses a glucose-modified 4H-beta-carboline carboxylic acid derivative and a preparation method thereof, and application of the derivative to preparation of an anti-thrombotic medicine. The invention also discloses a composition for preparing the anti-thrombotic medicine. The composition consists of an effective dose of compound shown as a general formula I and a pharmaceutically acceptable carrier or auxiliary material, wherein the compound accounts for 0.1 to 99 percent, preferably 10 to 60 percent of the total weight of the medicinal composition. The anti-platelet aggregation activity of the compound is evaluated by a common carotid artery-jugular vein extracorporeal circulation bypass thread model. Test results show that the compound has high anti-thrombotic activity and can be prepared into the anti-thrombotic medicinal composition and can be used for preparing the anti-thrombotic medicine.
CN103656626A Compound complexing calcium preparation for treating and nourishing bones for middle and old aged people and preparation method thereof The invention discloses a compound complexing calcium preparation for treating and nourishing bones for middle and old aged people and a preparation method thereof. The preparation is scientifically processed by a formula comprising deep sea fish bones, deep sea cuttle bones, biological calcium carbonate, tigris artifactus powder, collagen powder, vitamin K2, vitamin D, glucosamine, eucommia ulmoides, cordyceps sinensis, bovine coloctrum, magnesium, alpha-linolenic acid, xylitol and magnesium stearate. The formula of the invention is scientific in compatibility and reasonable in match of nutritional elements, and integrates the health-care effects of calcium supplement for bone-formation, calcium supplement for treating bones, calcium supplement for nourishing bones, calcium supplement for reinforcing bones, calcium supplement for improving the immunity and calcium supplement for enhancing the self-healing and rehabilitating capacity of the body. The preparation is remarkable in effect, high in clinical cure rate and excellent in contrast result with other calcium products clinically. The preparation is reasonable and feasible in process technology and is convenient to take by prilling and coating. The advanced, scientific and unique structure of the product is an advantage of the preparation.
US20090136463 Schwann Cell Bridge Implants and Phosphodiesterase Inhibitors to Stimulate CNS Nerve Regeneration The use of a composition that elevates intracellular levels of cyclic nucleotide cyclases in combination with phosphodiesterase inhibitors and cell grafts to restore function after CNS injury.
CN101365699A Pyrido(3,2-D)pyrimidines and pharmaceutical compositions useful for medical treatment This invention relates to substituted pyrido(3,2-d)pyrimidine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These derivatives are also useful in preventing or treating cardiovascular disorders, disorders of the central nervous system, TNF-alpha related disorders, viral diseases (including hepatitis C), erectile dysfunction and cell proliferative disorders.
US20050095663 Via 6-(4-chlorophenyl)-2-(2'-pentyn-4'-ene-1-yl)-3(2H)-pyridazinone for inhibition of delta-9 fatty acid desaturase Methods for identifying fungitoxic compounds are disclosed based on inhibition of the enzyme Δ-9 fatty acid de-saturase.
WO2013006548A3 Composition for use in treating and preventing inflammation related disorder The present invention is related to a use for treating and preventing inflammation related disorder of a composition containing a drug and hyaluronic acid (HA) or HA mixture, whereas the HA or the HA mixture as a delivery vehicle can be a formulation including at least two HAs having different average molecular weights. The composition has been demonstrated to be capable of reducing the therapeutic dose of a drug on the treatment and prevention of inflammation related disorders is acute inflammatory disease, chronic obstructed pulmonary disease, coeliac disease, conjunctivitis, otitis, allergic rhinitis, gingivitis, aphthous ulcer, bronchitis, gastroesophageal reflux disease (GERD), esophagitis, gastritis, enteritis, peptic ulcer, inflammatory bowel disease (IBD), Crohn's Disease, irritable bowel syndrome (IBS), intestinal inflammation or allergy, urethritis, cystitis, vaginitis, proctitis, eosinophilic gastroenteritis, or rheumatoid arthritis.
CN102898403A Method for preparing novel crystal form of 1-(bi(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxyphenyl)piperazine dihydrochloride The invention provides a method for preparing a novel crystal form of 1-(bi (4-fluorophenyl) methyl)-4-(2,3,4-trimethoxyphenyl) piperazine dihydrochloride. The method comprises the following steps of: completely dissolving lomerizine hydrochloride by using a solvent; and carrying out concentration, freeze-drying or volatilization to remove the solvent, wherein the solvent is one or a combination of multiple substances in alcohol solvents, acetonitrile or ether solvents. The method is simple in process and high in reproducibility, and the obtained novel crystal form has good pharmaceutical effect and high bioavailability.
WO2011098483A1 Pharmaceutical compositions comprising a combination of metformin and sitagliptin The present invention relates to a pharmaceutical composition, preferably a pharmaceutical dosage form, comprising at least two separate compartments, wherein one compartment contains a composition comprising metformin or a pharmaceutically acceptable salt thereof and wherein another compartment contains a composition comprising sitagliptin. The present invention also relates to a process for preparing dosage forms comprising metformin or a pharmaceutically acceptable salt thereof and sitagliptin or a pharmaceutically acceptable salt thereof, the process comprising the steps of: a) providing one composition containing metformin or a pharmaceutically acceptable salt thereof and optionally also sitagliptin, b) providing a further composition containing sitagliptin or a pharmaceutically acceptable salt thereof and optionally also metformin, and c) combining the compositions to form compartments. The present invention also refers to a process for preparing dosage forms comprising at least one compartment comprising metformin or a pharmaceutically acceptable salt thereof and sitagliptin or a pharmaceutically acceptable salt thereof, the process comprises providing a composition containing metformin or a pharmaceutically acceptable salt thereof, and sitagliptin or a pharmaceutically acceptable salt thereof, and a matrix agent. Moreover, the present invention related to a dosage form obtained by said process, and to the use of said dosage form for the treatment of diabetes.
CN102389436A Medicinal composition for resisting platelet aggregation The invention relates to a medicinal composition for resisting platelet aggregation. The medicinal composition is a solid preparation by using aspirin pharmaceutical salt and clopidogrel pharmaceutical salt as active components. The invention aims at making up the defects in the prior art, and supplies a novel preparation which has quick disintegration, fast absorption and convenient administration, and can improve bioavailability and blood concentration of the medicament, shorten the peak reaching time and improve platelet aggregation resistance to broad patients and medical staff. The oral solid preparation is prepared by using aspirin pharmaceutical salt and clopidogrel pharmaceutical salt as raw materials, and adding auxiliary materials with certain specific varieties and proportions according to a pharmaceutical conventional technology.
US20120114625 Shelf-stable fermented dairy products and methods of making same Shelf-stable fermented dairy products and methods of making the shelf-stable fermented dairy products are provided. The shelf-stable fermented dairy products can be shelf-stable with improved taste, viscosity and texture profiles. In a general embodiment, the present disclosure provides a shelf-stable fermented dairy product including a shelf-stable fermented dairy component, a stabilizer, and a puree composition. The shelf-stable fermented dairy component can be, for example, yogurt, sour cream, buttermilk or a combination thereof.
WO2007138233A2 Use of zatosetron for the treatment of rosacea, and pharmaceutical compositions The invention relates to the use of zatosetron or the salts thereof as an active substance in a pharmaceutical composition, especially a dermatological composition. The composition is preferably topically applied and is used for the treatment and/or prevention of rosacea.
WO2009066774A1 Selective expression inhibitor for aurora kinase a and aurora kinase b genes A drug containing a pyrrole-imidazole polyamide comprising an N-methylpyrrole unit (hereinafter sometimes referred to as Py), an N-methylimidazole unit (hereinafter sometimes referred to as Im) and a γ-aminobutyric acid unit which can be folded at the γ-aminobutyric acid unit to form a U-shape conformation within the minor groove in the double strand region (hereinafter referred to as the target region) containing a part of the -100 to -70 positions (SEQ ID NO:2) in the base sequence of human aurora kinase A (hereinafter sometimes referred to as hAURKA) promoter or the whole thereof and a chain that is complementary thereto, and in which the C-G base pair corresponds to the Py/Im pair, the G-C base pair corresponds to the Im/Py pair and the A-T and T-A base pairs correspond each to the Py/Py pair.
US20100113450 Agent for Preventing and Alleviating Wrinkles The present invention provides an agent for preventing and alleviating wrinkles which has excellent effects of preventing and alleviating wrinkles formed by decreased barrier function of the skin owing to aging or photo aging, that is graphic wrinkles or linear wrinkles. The agent for preventing and alleviating wrinkles consisting of one or more compounds selected from the group consisting of gamma-aminobutyric acid derivatives represented by the following formula (1) or N,N,N-trimethyl gamma-aminobutyric acid represented by the following formula (3) and salts thereof: wherein R1 and R2 independently represent any of a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a benzyloxycarbonyl group, a cyclohexyl group, a cyclohexanemethyl group, a cyclohexanecarbonyl group, a guanidino group formed with nitrogen atom in the formula (1), an ureido group formed with nitrogen atom in the formula (1), and a group represented by following formula (2). Additionally, R1 and R2 may jointly form a piperidine ring, morpholine ring, or pyrrolidine ring. Both of R1 and R2 are not simultaneously a hydrogen atom.
CN102389435A Application of pseudojujubogenin to preparation of medicaments for resisting senile dementia The invention provides application of pseudojujubogenin to preparation of medicaments for resisting senile dementia. The pseudojujubogenin is shown as a structural formula. Through research on influence of the pseudojujubogenin on mouse memory acquisition impairment caused by scopolamine, the memory acquisition impairment can be improved when the pseudojujubogenin is orally taken by a mouse in ratios of 150 mg/kg, 50 mg/kg, and 15 mg/kg; a mouse suffering from focal cerebral ischemic-reperfusion injury can be protected when the pseudojujubogenin is taken by the mouse in ratios of 35 mg/kg, 15mg/kg, and 5 mg/kg; and memory impairment of APP/PS1 double transgenic mice can be obviously improved when the pseudojujubogenin is taken by the mouse in ratios of 50 mg/kg and 15mg/kg. Therefore, the pseudojujubogenin can be used for preparing the medicaments for resisting the senile dementia and has great clinical application value.
CN101884632A Compound preparation prepared from oseltamivir and ascorbic acid The invention relates to a novel viral influenza treating medicine, in particular to a compound preparation prepared form oseltamivir as a neuraminidase inhibitor and ascorbic acid as a cell membrane protector. The chemical name of oseltamivir is (3R, 4R, 5S)-4-acetamide-5-amino-3(1-ethyl propoxy)-1-cyclohexene-ethyl carbonate. Ascorbic acid is used for protecting cell membrane in order to overcome the serious toxic and side effects of the traditional neuraminidase inhibitor. A negative potential exists on the external surface of a healthy human cell, ascorbic acid is an efficient negative-charge carrying molecule, can efficiently inhibit the combination of human neuraminidase with oseltamivir and can reduce the toxic and side effects of oseltamivir on the nervous system.
WO2011150094A3 Tumor suppression compositions Provided herein is tumor suppression composition and methods of making and using the same.
CN103360403A Compound having cytotoxicity, composition, and preparation method and use thereof The invention relates to a compound having cytotoxicity, composition, and a preparation method and use thereof. The invention relates to a compound as described in formula (I) in the description, and medically acceptable salts, solvates or hydrates thereof, a preparation method thereof, and a composition containing the compound. The invention also provides the use of the compound in the prevention and/or treatment of cancers. The invention also provides an extract of monascus fermentation products and the use thereof in the prevention and/or treatment of cancers.
US20120028958 5-alkynyl-pyrimidines The present invention encompasses compounds of general formula (1) wherein R1 to R4 R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
EP1851234B1 Substituted propane phosphinic acid esters The present invention relates to certain esters of substituted 3-aminopropane phosphinic acid derivatives of formula I as disclosed herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
US8034817 Inhalation of quinolinonecarboxylic acid compound The invention relates to inhalable quinolonecarboxylic acid derivative compositions for local control of diseases of the respiratory organs, in particular of lung diseases.
EP1693373A1 Enantiomerically pure beta-D-(-)-dioxolane-nucleosides The present invention provides enantiomerically pure β-D-(-)-dioxolane-nucleosides. The enantiomerically pure dioxolane nucleosides are active HIV agents, that are significantly more effective than the prior prepared racemic mixtures of the nucleosides.
CN102499902A Oral cavity care composition The invention provides an oral cavity care composition which contains vitamin C and pearl hydrolysate which is prepared from sea pearl by a biochemical method. The oral cavity care composition can be applied to toothpaste, gel, mouth wash, powder, candy, lozenge and other oral cavity care products. The vitamin C and the pearl hydrolysate can be used together for improving the stability of the composition in a product shelf life, and can act synergistically to promote absorption, and have the effects of nourishing teeth and gum, caring oral cavity, strengthening gum and firming teeth, which are superior to those of a single active matter.
US7977466 C-glycoside derivatives and salts thereof The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
US20090221697 Macrolide conjugates of pyrrolizine and indolizine compounds as inhibitors of 5-lipooxygenase and cyclooxygenase The present invention relates to macrolide conjugates of pyrrolizine and indolizine derivatives with macrocyclic antibiotics and derivatives thereof. The macrolide conjugates are potent inhibitors of 5-lipoxygenase and cyclooxygenase and are therefore suitable to treat disorders of the rheumatic type and to prevent allergically induced diseases. The macrolide conjugates have significantly enhanced potency and efficacy.
US20090281179 Carbamate compounds for use in preventing or treating neuropathic pain and cluster and migraine headache associated pain This invention is directed to a method for preventing or treating neuropathic pain and cluster and migraine headache-associated pain comprising administering to a subject in need thereof a therapeutically effective amount of an enantiomer of Formula (I) substantially free of other enantiomers or an enantiomeric mixture wherein an enantiomer of Formula (I) predominates: wherein phenyl is substituted at X with one to five halogen atoms independently selected from the group consisting of fluorine, chlorine, bromine and iodine; and; R1 and R2 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).
WO2010015520A1 Substituted naphthyridines and use thereof as medicines The invention relates to novel substituted naphthyridines of the formula (1) and to pharmacologically compatible salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, where R2 and where R1 can be a radical A or R1 can be a radical B as described in claim 1 and where R3, R4, R5, R6, R6', R7, R8, R9, R10, V, n and m can have the meanings indicated in claim 1, and pharmaceutical compositions containing these compounds.
CN102812007A Therapeutic agent for hepatitis C Provided is a therapeutic agent for hepatitis C. A compound that has anti-HCV activity, which is useful in the treatment of hepatitis C, is an active ingredient of said agent. Said compound is the compound represented by formula (I) or a pharmacologically-permitted salt thereof.
US20100267769 Substituted Bicyclocarboxyamide Compounds This invention provides a compound of the formula These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.
CN101951918A Treating hyperglycemia with 25-hydroxyvitamin D3 We disclose treating hyperglycemia in a human with 25-hydroxyvitamin D3 (calcifediol). Blood glucose is reduced to a level which is closer to normal than baseline. Vitamin D3 (cholecalciferol) may optionally be used together with 25-hydroxy vitamin D3. Forms and dosages of a pharmaceutical composition, as well as processes for manufacturing medicaments, are also disclosed.
CA2392570C 4-pyrimidinyl-n-acyl-l-phenylalanines Coumpounds of Formula (1) are disclosed, wherein R1 to R6 are as defined in specification and which are inhibitors of binding between VCAM-1 and cells expressing VLA-4, and accordingly are useful for treating diseases whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
US7074412 For therapy of orthopaedic and dental, including periodontal, diseases The present invention relates to pharmaceutical compositions containing a synergistic amount of at least one bone morphogenetic protein (BMP) and a synergistic amount of at least one pyrrolidone optionally in a pharmaceutically acceptable carrier, such as a biodegradable polymer. The present invention further relates to methods of treating orthopaedic and dental, including periodontal, diseases by simultaneously administering a synergistic amount of at least one bone morphogenetic protein (BMP) and a synergistic amount of at least one pyrrolidone optionally in a pharmaceutically acceptable carrier to patients in need of such treatment.
WO2014042605A1 New tiotropium bromide crystalline form The present invention is related to crystalline compound comprising Tiotropium bromide and the process that shall be used in production of said compound.
CN102892757A Phenol derivatives and the pharmaceutical or cosmetic use thereof The invention relates to novel compounds having general formula (I) and the cosmetic or pharmaceutical use thereof.
EP2455080A1 S1P1 receptor agonists for use in the treatment of multiple sclerosis a S1 P1 receptor agonist of formula (I), or a pharmaceutically acceptable salt, or solvate, or N-oxide, or stereoisomer or deuterated derivate thereof, alone or combined with IFNβ, for use in the treatment of multiple sclerosis disease.
US20070020275 Nucleic acid sequences of hyperplasia and tumours of the thyroid The invention relates to a nucleic acid which codes for a polypeptide. Said polypeptide comprises a KRAB domain and/or at least one zinc finger motif, whereby the KRAB domain contains the amino acid sequence of SEQ ID NO: 1 and the zinc finger motif is of the type contained in the zinc finger domain with the amino acid sequence of SEQ ID NO: 2.
CN101116747A Cytosine arabinoside and gland correlated virus composite preparations and uses thereof The invention belongs to the biologic medicine filed and relates to a novel gene therapy compound preparation and the use and application method thereof. When adeno-associated virus is used as gene delivery carrier, a certain dose of cytarabine is combined in use, and obviously increases transfer efficiency of normal cells and tumor cells by the adeno-associated virus, advances expression time of foreign gene mediated by adeno-associated virus, obviously increases positive rate and expression level, thereby improving the gene therapy effect employing adeno-associated virus as carrier, particularly the application in gene therapy for diseases, such as ocular fundus disease, genetic disease and tumor. In tumor gene therapy, the invention has functions of inhibiting tumor cell growth, inducing tumor cell apoptosis, and obviously increases the transfer efficiency and expression level of the gene mediated by adeno-associated virus.
US20050274671 Method for preparing a compound of interaction of active substances with a porous support using supercritical fluid The invention concerns a method for preparing compounds for interaction of an active substance hardly soluble in an aqueous medium with a porous support. The invention is characterized in that it comprises the following steps: (a) mixing the active substance generated by supercritical fluid and the specific amount of porous support; (b) carrying out a molecular diffusion step by contacting in static mode a supercritical fluid with the mixture obtained at step (a) for the time required to improve the dissolution in the aqueous medium of the mixture obtained at step (a); (c) washing the interactive compound obtained at step (b) with a supercritical fluid flow; (d) recuperating the particles of the interactive compound thus formed. The invention also concerns a compound obtainable by said method.
US20090082396 5-aryl-4,5-dihydro-(1h)-pyrazolines as cannabinoid cb1 receptor agonists The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor agonists, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, administered to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. Compounds of the present invention include compounds of formula (I): wherein the substituents have the definitions given in the specification.
CN101732268A Montelukast sodium tablet and preparation method thereof The invention belongs to the field of medicine preparations, in particular to a montelukast sodium tablet and a preparation method thereof. Because the montelukast sodium tablet adopts a wet method granulation process and has the problems of long drying time, difficult temperature control and easy causing of content difference, content descent and relevant substance increase between particles, the invention provides the montelukast sodium tablet and the preparation method thereof in order to enhance the stability and the operability of the montelukast sodium tablet. The montelukast sodium tablet provided by the invention comprises montelukast sodium, a filling agent, a disintegrating agent, an adhesive, a colorant, a lubricant and a flow aid. The preparation method of the montelukast sodium tablet provided by the invention adopts direct tabletting after dry method granulation and uses the colorant, the colorant can act as a very good light shielding function in the operational process, the operation is convenient, the influence of a drying process and moist heat to the product quality is avoided, and the product stability is enhanced.
CN101967193A Hsp60 fragment capable of being combined with LOX-1, derivatives thereof and use thereof The invention provides an Hsp60 fragment capable of being combined with LOX-1, derivatives thereof and use thereof. The derivatives comprise fusion protein, compounds, composites and the like. Particularly the invention relates to a discovery that LOX-1serves as a coreceptor of an Hsp60 family and mediates the combination and internalization of the Hsp60 by identifying the C terminal of the Hsp60. The immune effect of an antigen fused with the C terminal of the Hsp60 can be improved by LOX-1. The Hsp60 fragment provides a theoretical basis for further researches on the biological functions of Hsp60 and research and development of anti-tumor immunity and anti-infectious agent by using Hsp60 and the C terminal of the Hsp60 as a vaccine delivering tool and LOX-1 as a receptor target.
US20110293691 Multimodal adhesion barrier Provided herein are multimodal barrier materials useful for preventing adhesions in a subject, which may include a collagen, a collagen deposition inhibitor and/or a chitosan.
CN1850073A Medicinal composition containing ampicillin and its preparing method The present invention belongs to the field of medicine product, in particular, it relates to a medicine composition for raising bioavailability of ampicillin solid preparation and its preparation method. Said medicine composition mainly is composed of ampicillin and piperine, their weight ratio is 1:0.012-1:0.03. Said invention also provides the concrete steps of its preparation method.
WO2010009288A1 Compositions and uses of antiviral active pharmaceutical agents Several embodiments of the present invention provide for a method of treating, reducing or minimizing asthma exacerbations in humans that are PCR+ for a rhinovirus, which includes orally inhaling or intranasally administering a therapeutically effective amount of pleconaril.
WO2011143590A1 Combination therapy compositions and methods using lipoic acid derivatives and an anti-proliferation agent The invention provides combination therapy compositions, therapeutic methods, and kits for use in treating cell proliferation disorders, such as cancer. The combination therapy involves administering a redox-modulating compound, such as a lipoic acid derivative, in combination with an anti-proliferation agent, such as gemcitabine
US20090029960 Macrocyclic compounds useful as base inhibitors The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
US20120171279 Strongly bound base-modified oligonucleotides The present invention provides compounds having a chelating moiety and an oligonucleotide sequence wherein the oligonucleotide includes one or more modified nucleobases, such as hydroxynucleobases. The disclosed compounds are suitable for antisense therapy. The chelating moiety can be complexed to an ion of a lanthanide metal. These compounds are efficient translation inhibitors of nucleic acids and have increased binding affinity for target nucleic acids. The invention also includes compositions and methods of using these compositions as antisense therapy.
US20050137242 Betamimetics having a long-lasting activity, processes for preparing them, and their use as medicaments A compound of formula 1 wherein: R1 is a group wherein R3 is a benzyl group optionally substituted by a methoxy group; R4 is a hydrogen atom, or R3 and R4 together are a —CO—CH2—O— bridge, the carbonyl group of the bridge being bound to the nitrogen; and R2 is a group selected from wherein R5 is a dimethylamino, methoxy, or butoxy group, X is a nitrogen or a carbon atom, and R6 is a methoxyphenyl group, if X is nitrogen, or is an anellated phenyl ring also linked to X, if X is carbon, or the individual optical isomers, mixtures of the individual enantiomers, racemates, or acid addition salt thereof.
US7247502 Nicotine hapten that is nicotine in which the pyrrolidine ring is substituted by an omega-carboxy-, -amino-, -formyl- or -mercapto-alkyl group; useful in formulating vaccines for active immunization Novel hapten-carrier conjugates are capable of inducing the production of antibodies, in vivo, that specifically bind to nicotine. These conjugates comprise a nicotine hapten conjugated to an immunogenic carrier protein. The novel conjugates preserve the chirality of nicotine in its native (S)-(−) state, and have good stability properties. The conjugates are useful in formulating vaccines for active immunization, that are used to prevent and treat nicotine addiction. The antibodies raised in response to the nicotine hapten-carrier conjugate are used for passive immunization. These antibodies are administered for prevention and treatment of nicotine addiction.
EP1392643B1 Trisubstituted-n- (1s)-1,2,3,4-tetrahydro-1-naphthalenyl] benzamides which inhibit p2x3 and p2x2/3 containing receptors Compounds of formula (I), are novel P2X3 and P2X2/P2X3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.
US7910591 e.g. 3-[4-(4-Pyridine-2-yl-piperazine-1-yl)-butyl]-1,3-dihydro-2H-indol-2-one; serotonin 5-HT7 and alpha 1 receptors modulator; antxiolytic agent, antidepressant; neurodegenerative diseases; schizophrenia, Alzheimer's disease, stroke, dementias; side effect reduction The present invention is concerned with new indol-2-one derivatives of Formula (I), which have favorable activity profile for the prophylaxis and treatment of disorders in the central nervous or in the cadiovascular system.
US20110160232 Certain chemical entities and therapeutic uses thereof Certain chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with PB kinase activity are described.
US6858581 Peptides which are modified with at least one hydrocarbyl group and which possess antimicrobial acitivity Compositions and methods for inhibiting and controlling the growth of microbes are disclosed. The composition comprises at least one chemically-modified peptide with antimicrobial activity and at least one carrier. The method comprises of administering an amount, effective for the prevention, inhibition and termination of microbial growth for industrial, pharmaceutical, household and personal care use.
CN101671351A Carbon 2-bit substituted cephalosporin derivative as well as synthetic method and application thereof The invention relates to a carbon 2-bit substituted cephalosporin derivative as well as a synthetic method and application thereof. The synthetic method comprises the following steps: carrying out Mannich condensation by taking GCLE and derivatives thereof as raw materials to introduce double bonds and a methylation reaction, carrying out Michael addition reaction based on the Manich condensationto modify cephalosporin mother nucleus 2-bit, thereby acquiring a series of compounds. The acquired target compounds have a certain antibacterial activity to gram-positive bacteria, wherein two compounds with the form of sulphoxide in 1-bit also present stronger combination ability with beta-lactamase.
CN1984658A Opioids for the treatment of the chronic obstructive pulmonary disease (COPD) The present invention relates to an opioid controlled release oral dosage form comprising at least one opioid for the manufacture of a medicament to treat patients with Chronic Obstructive Pulmonary Disease (COPD).
WO2009061271A1 Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase The invention provides certain novel 6-heteroaryl-5-methyl-3- oxo-4- [3 (trif luoromethyl) phenyl] -3,4-dihydropyrazine-2- carboxamide derivatives and pharmaceutically acceptable salts thereof and particular Forms thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitord of human neutrophil elastase.
CN102020645A Pyrazolopyrimidinone derivatives and pharmaceutical salts, preparation method and application thereof The invention relates to pyrazolopyrimidinone derivatives and pharmaceutical salts shown in a formula (I), a preparation method and application thereof, wherein R1 is selected from H or alkoxy, and R2 is selected from alkyl. The pyrazolopyrimidinone derivatives or pharmaceutical salts thereof have the function of inhibiting phosphodiesterase V, and can be used for preparing treating medicines fortreating male impotence, pulmonary hypertension, urethralsyndrome, benign swollen prostate, chronic heart failure, apoplexia, coronary artery disease, nervous pituitary diseases and the like.
US20130029981 Compounds, compositions, and methods for controlling biofilms The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.
WO2014134510A1 Glycopyrrolate salts Salts of glycopyrrolate, including solid forms and formulations such as topicals thereof, are disclosed. Methods of making glycopyrrolate salts, including formulations such as topicals thereof, and methods of treating hyperhidrosis with salts of glycopyrrolate, and formulations such as topicals thereof, are disclosed.
CN1672680A Stable moxixacin tablet and its prepn process The present invention relates to stable moxixacin tablet and its preparation process. The preparation contains moxixacin or its salt and/or hydrate and tablet supplementary material. The present invention features that during preparation, hypromellose or other filming material may be added to prepare granule before tabletting so that the medicine is stable without color change during pelletizing and tabletting.
US20100273856 Screening of micro-rna cluster inhibitor pools The disclosure provides methods for inhibiting the activity of a miRNA cluster in a cell, and also for screening a cell for a phenotype(s) of interest resulting from inhibition of a miRNA cluster. The methods use a cluster pool which comprises at least one miRNA inhibitor specific for each miRNA in the miRNA cluster. MiRNA inhibitors are described that induce apoptosis in breast cancer cells and hence are useful in the treatment of breast cancer. The disclosure also provides pharmaceutical compositions which are useful for the treatment of breast cancer; methods for inducing the nuclear translocation of NF-κB in a breast cancer cell; methods for inducing the nuclear translocation of c-Jun in a breast cancer cell; method for inhibiting the nuclear translocation of NF-κB in a breast cancer cell; and methods for providing prognostic medical information relating to breast cancer progression.
US20100151051 Anti-tumor drug, medicament, composition, and use thereof An active polypeptide comprising the amino acid sequence of SEQ ID NO:4, having an anti-tumour activity, and compositions and methods including the active polypeptide.
WO2009062374A1 The pharmaceutical use of liquiritigenin for preparing medicine for treating neurodegenerative diseases The pharmaceutical use of Liquiritigenin and the composition containing Liquiritigenin is provided for treating neurodegenerative diseases, particularly senile dementia or Parkinson's disease .
US20080194617 Fused ring compound The present invention provides an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like. The present invention relates an agent for the prophylaxis or treatment of diabetes, which comprises a compound represented by wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.
WO2011068978A1 Methanocarba adenosine derivatives and dendrimer conjugates thereof Disclosed are (N)-methanocarba adenine nucleosides, e.g., of the formula (I): as A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein A, a, R2, and R3 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. Also disclosed are conjugates comprising a dendrimer and one or more ligands, which are functionalized congeners of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily. Such conjugates are have the potential of being used as dual agonists, dual antagonists, or agonist/antagonist combinations.
EP1064402B1 Antisense modulation of lfa-3 Compositions and methods for the treatment and diagnosis of diseases or disorders amenable to treatment through modulation of expression of a nucleic acid encoding a lymphocyte function associated antigen 3 (LFA-3; also known as CD58) protein are provided.
US20070031480 Enhanced delivery of sphingolipids Compositions which comprise delivery vehicles having stably associated therewith at least one organic acid derivative of a sterol are useful in achieving enhanced cellular delivery of physiologically relevant sphingolipids when the compositions are administered.
CN102688205A Preparation method of esomeprazole sodium for injection The invention discloses a preparation method of esomeprazole sodium for injection. The method is characterized in that: the proppant and stabilizer in the formula of the esomeprazole sodium for injection are optimized, and the spray pre-freezing and microwave freeze-drying technologies are adopted for drying; and the production period is shortened, the energy consumption is reduced, the cost is lowered, the product quality is guaranteed, the product stability is enhanced, and a satisfactory effect is achieved.
US20120149737 Therapeutic Aryl-Amido-Aryl Compounds and Their Use The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, are (selective) retinoic acid receptor α (RARα) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RARα, and in the treatment of diseases and conditions that are mediated by RARα, that are ameliorated by the activation of RARα, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment.
WO2011126810A3 Intravaginal drug delivery device Described herein is an intravaginal drug delivery system. In an embodiment the intravaginal drug delivery system includes a progestin and estrogen compound, and releases the active ingredients in a fixed physiological ratio over a prolonged period of time to produce a contraceptive state in a female.
WO2008113456A1 Tetrahydroquinoline derivatives and use of same for treating cancer The invention relates to compounds of formula (I) wherein E, R3, R4, R5, X, Y, W, Q1, Q2, Z, s and m have the designations cited in claim 1. Said compounds can be used, inter alia, for the treatment of tumours.
CN101838254A L-arginine derivative epimedium herb flavone combination and preparation method thereof The invention provides an L-arginine derivative epimedium herb flavone combination with a general formula (III), a preparation method and application thereof. The combination has prominent pharmacological activities on osteoporosis and bone metabolic diseases because of synergistic effects of two kinds of pharmacological mechanisms. The synthesis method has the advantages of high yield, high synthesis speed, and easy purification of products.
US20120070470 Hemostatic compositions, devices, and methods Compositions that include a clay such as kaolin dispersed in a liquid such as water may be useful for promoting the clotting of blood. The compositions may be in a liquid, gel, paste, foam, or another form. Uses may include treating a traumatic injury such as in injury caused by a bullet, an explosive, a blade etc., or an injury caused during a medical procedure such as surgery.
WO2014050134A1 Therapeutic agent for dyslipidemia The present invention addresses the problem of providing a pharmaceutical combination composition and drug combinations for the prevention and/or treatment of dyslipidemic conditions such as atherosclerosis, hypercholesterolemia, low HDL blood disease in mammals including humans. A pharmaceutical composition for the prevention and/or treatment of dyslipidemia, etc. which comprises (a) a compound represented by general formula (1) (in the formula, each symbol is the same as defined in the specification) or a salt thereof or a solvate thereof and (b) a cholesterol absorption inhibitor. (1)
CN102846562A Galactose-mediated oridonin albumin nanoparticle and preparation method thereof The invention discloses a galactose-mediated oridonin albumin nanoparticle, which is prepared from the raw material and auxiliary materials, wherein the raw material is oridonin; the auxiliary materials consist of galactosylation albumin, crosslinking agent, cryoprotectant and water; the mass ratio of the use amount of the raw material and the auxiliary materials is as follows: by 10ml of nanoparticle preparation, the oridonin is 2.0-40.0mg, the galactosylation albumin is 50.0-400.0mg, the crosslinking agent is 0.4-8.4mg, the cryoprotectant is 0 or 0.1-0.5g, and the balance is water. The galactose-mediated oridonin albumin nanoparticle disclosed by the invention has a good biocompatibility. After the galactose-mediated oridonin albumin nanoparticle is made into injection-purpose nanometer solution, the bioavailability of the medicine is favorably increased, the medicine administration dose is reduced, the toxic and side effect is lowered, and the purpose on changing the in-vivo distribution of the medicine, prolonging the medicine acting time and improving the bioavailability can be achieved. The preparation method is simple and easy to realize and is suitable for large-scale production.
US20100016249 Cancer sensitizer comprising glucosamine, glucosamine derivatives or salts thereof Disclosed herein is a cancer sensitizer comprising glucosamine, a glucosamine derivative, or a salt thereof. When administered to patients with cancer, the cancer sensitizer functions to sensitize cancer cells to anticancer agents without producing side effects, thereby increasing the therapeutic efficiency of chemotherapy.
EP1509498B1 Pentafluorosulfanyl-benzoylguanidine, method for the production thereof and its utilization as medicament or diagnostic agent and medicament containing same The invention relates to pentafluorosulfanyl-benzoylguanidines of formula (I) and (II), wherein R1 to R4 have the meaning mentioned in the claims. Said pentafluorosulfanyl-benzoylguanidines are suitable as antiarrhythmic medicaments with cardioprotective components for the prophylaxis or treatment of infarction and for the treatment of angina pectoris. They also preventively inhibit pathophysiological processes during the occurrence of ischaemically induced injuries, more particularly the triggering of ischaemically induced cardiac arrhythmia.
US6909000 Inhibiting particularly the activity of hepatitis C virus NS3-NS4A protease; peptidomimetics having a bridged bicyclic moiety at the P2 position. The present invention relates to peptidomimetic compounds which inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The compounds of this invention have a bridged bicyclic moiety at the P2 position. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.
CN101862469A Chitosan derivative quick hemostasis granules and preparation method thereof The invention discloses a chitosan derivative quick hemostasis granules and a preparation method thereof. The hemostasis granules are prepared by mixing chitosan hydrochloride, O- carboxymethyl chitosan and auxiliary material with purified water according to a certain proportion, sufficiently stirring and uniformly blending, adding ammonia to adjust the pH value of the mixed liquor to 7.0-9.0, carrying out vacuum filtration, and carrying out aseptic spray drying on the filtrate. The hitosan derivative quick hemostasis granules have the pH value suitable for the body fluid of a human body, haslittle irritation to the skin, can quickly stanch, has the functions of easing pain, promoting wound healing, inhibiting bacteria and the like, and is suitable for various wound hemostasis emergency treatments of trauma haemorrhage, including the hemostasis of large-area haemorrhage. In addition, the preparation method is simple and is easy for scale production.
EP2484669A1 Novel phenol derivative Disclosed are a novel compound and a pharmaceutical product, each having a remarkable uricosuric effect. Specifically disclosed are: a novel phenol derivative represented by general formula (1) that is shown in Fig. 1; a pharmaceutically acceptable salt thereof; a hydrate of the derivative or the salt; and a solvate of the derivative or the salt. (In the formula, R1 and R2 may be the same or different and each represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group, a haloalkyl group, a haloalkoxy group, an alkylsulfanyl group, an alkylsulfinyl group, an alkylsulfonyl group, a lower alkyl-substituted carbamoyl group, a saturated nitrogen-containing heterocyclic N-carbonyl group, a halogen atom, a cyano group or a hydrogen atom; R3 represents a lower alkyl group, a haloalkyl group, a halogen atom, a hydroxy group or a hydrogen atom; and X represents a sulfur atom, an -S(=O)- group or an -S(=O)2-group.)
US20100234379 Dual modulation of endocannabinoid transport and fatty-acid amide hydrolase for treatment of excitotoxicity The endocannabinoid transporter and FAAH are sites of modulation that allow pharmacological enhancement of protective endocannabinergic signals. Selective inhibitors of the transporter and inhibitors of FAAH caused additive augmentation of endogenous signaling events mediated by the cannabinoid CB1 receptor. Disruption of such signals has been shown to prevent neuronal maintenance processes and increase vulnerability to brain damage. Here, blocking endocannabinoid inactivation enhanced cannabinergic activity and ameliorated cellular disturbances associated with excitotoxicity. Modulating the endocannabinoid system in this way also prevented excitotoxic behavioral abnormalities including memory impairment. Collectively, these results indicate that increasing endocannabinoid responses by inhibiting the endocannabinoid transported and/or the inhibiting FAAH leads to molecular, cellular, and functional protection against excitotoxic insults like stroke and traumatic brain injury.
WO2008147826A1 Malaria liver stage drugs The invention provides methods for inhibiting the growth of liver stage Plasmodium parasites using inhibitors of apicoplast fatty acid synthesis. The invention further provides methods for preventing malaria and methods for treating Plasmodium infections.
WO2013007766A1 Means and methods for the treatment of pathological angiogenesis The present invention has found that inhibitors reducing the glycolytic flux are not only useful for the treatment of cancer but can also be applied for the treatment of pathological angiogenesis such as for example macular degeneration. In particular the invention provides siRNAs directed against PFKFB3 for the treatment of pathological angiogenesis. The invention also provides the use of a therapeutically effective amount of aza chalcones or a pharmaceutically acceptable salt thereof for the treatment of pathological angiogenesis such as for example macular degeneration.
US20120322860 Aptamer therapeutics useful in the treatment of complement-related disorders The invention provides nucleic acid therapeutics and methods for using these nucleic acid therapeutics in the treatment of complement-related disorders.
EP2233143A1 Use of idrabiotaparinux for decreasing the incidence of bleedings during an antithrombotic treatment The invention relates to the use of idrabiotaparinux for the treatment and secondary prevention of thrombotic pathologies, wherein the use of idrabiotaparinux involves a decrease in the incidence of bleedings, in particular major bleedings, during said treatment.
US20120052122 Treatment Of Chronic Obstructive Pulmonary Disease With Phosphodiesterase-4 Inhibitor Disclosed is a method of treatment of chronic obstructive pulmonary disease associated with chronic bronchitis in a patient at risk of exacerbations. The method includes administering to a patient with a history of chronic obstructive pulmonary disease associated with chronic bronchitis and at risk of exacerbations, a maintenance dose of 500 micrograms per day of roflumilast. Also disclosed is a method of increasing pre-bronchodilator FEV1 or post-bronchodilator FEV1 in such a patient, and increasing pre-bronchodilator FVC or post-bronchodilator FVC in such a patient. Further disclosed is a method of reducing the rate of exacerbations in such a patient.
WO2013126156A1 Nitric oxide donating selective glucocorticoid receptor agonist compounds and ophthalmic compositions A compound and composition useful in the treatment of ocular inflammation or prevention of glaucoma or its progression comprising a nitric oxide donating selective glucocorticoid receptor agonist ("NO donating SEGRA"), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can comprise an additional anti-inflammatory agent and can be formulated for topical application, injection, or implantation. It may be used in combination with another therapy directed to reducing intraocular pressure or ocular inflammation.
CN102309479A Application of isoflavone compound in preparation of medicaments or foods for resisting tumors The invention relates to the field of pharmacy and medical technology and particularly relates to application of an isoflavone compound (irisflorentin) from Belamcanda chinensis (L.)DC. in the preparation of medicaments or foods for resisting tumors. Proven by in-vitro experiments, the isoflavone compound has an effect of obvious inhibiting the growth of cell strains A549 (human lung cancer cell), LOVO (human colon cancer cell), 6T-CEM (human Tcell leukemic cell) and HL-60 (human leukemic cell), therefore the isoflavone compound can be used for preparing the medicaments or foods for resisting tumors. The invention provides a new source for preparing the medicaments or foods for resisting tumors.
CN102552934A Adriamycin nano-particles and preparation method thereof The invention provides adriamycin nano-particles. The adriamycin nano-particles are prepared by compounding adriamycin and a block copolymer with a structure shown as a formula (I) or a formula (II) through electrostatic interaction. A preparation method for the adriamycin nano-particles comprises the following step of: electrostatically compounding the adriamycin and the block copolymer with thestructure shown as the formula (I) or the formula (II) in an aqueous medium to obtain the adriamycin nano-particles. In the aqueous medium, a poly(gamma-propargyl-L-glutamate-g-mercaptosuccinic acid)segment and a polyethylene glycol segment which are contained in the block copolymer wrap the adriamycin into cores of the nano-particles, so the adriamycin composite particles are high in stability.The nano-particles are expected to be gathered at tumor sites in blood circulation through an 'enhanced permeability and retention effect' so as to improve the targeting effect of the adriamycin on the tumor sites. Meanwhile, the electrostatic interaction between a carboxyl group of the block copolymer and an amino group of the adriamycin is easy to eliminate under the condition of low intracellular pH values, so that the intracellular release can be accelerated, and the medicinal effect can be improved.
WO2014035070A1 Composition for preventing or treating kidney disease comprising pyrazole derivative The present invention provides a composition for preventing or treating kidney disease, the composition comprising a pyrazole derivative compound or a pharmaceutically acceptable salt thereof; and the composition of the present invention is effective in reducing proteinuria, reducing cell formation between glomerular blood vessels and suppressing kidney fibrosis.
WO2013075399A1 Unsaturated 5-membered benzo-heterocyclic compound or pharmaceutical salts thereof, and preparation method, pharmaceutical composition and use thereof Provided in the present invention are an unsaturated 5-membered benzo-heterocyclic compound with the structure as shown in general formula I or pharmaceutical salts thereof, and a preparation method, a pharmaceutical composition and the use thereof. Experiments have shown that the compound of the present invention has the effects of upregulating the expression activity of bone morphogenetic protein BMP-2 and anti-osteoporosis in vivo, and also has the effect of improving SAMP6 mice osteoporosis symptoms. Activity tests in vitro have shown that the compound of the present invention shows an obvious upregulation effect on bone morphogenetic protein BMP-2.
WO2008043148A1 The use of a dna damaging agent and a ligand for the treatment of cancer The present invention relates generally to a method of treating a neoplastic condition and to agents useful for same. More particularly, the present invention is directed to a method of facilitating the treatment of a metastatic neoplastic tumour in a localised manner by effecting the exposure of neoplastic cell intra-cellular molecules, preferably intra-nuclear molecules, suitable for use as a therapeutic target. The co-localisation of tumour cells and metastases to discrete tissue locations thereby renders the method of the present invention useful in terms of the delivery of bystander-based therapy.
EP1937363A2 Use of compounds comprising fatty acid entities The invention comprises the use of compounds comprising non β-oxidizable fatty acid entities according to formula (I) or (II) for the preparation of a pharmaceutical composition for the prevention and/or treatment of conditions associated with low/decreased bone mineral density (BMD), and/or for increasing the BMD by decreasing the bone resorption.
CA2370323C Preparation for veterinary use for the prevention of ear diseases Preparation for veterinary use suitable for ear hygiene and for the prevention of ear diseases which includes at least one keratolytic and cerumenolytic cleaning agent selected from lactic acid, salicylic acid or a mixture of both, one bactericide agent, one yeast control agent and one anti-irritant and anti-pruriginous agent. Furthermore, it may include at least one agent that enhances its cerumenolytic properties, at least one vegetable extract with antiseptic and cicatrizant properties and/or at least one deodorant agent.
US20110091377 Biomarkers for melanoma The present invention relates to methods of determining melanoma status in a subject. The invention also relates to kits for determining melanoma status in a subject. The invention further relates to methods of identifying biomarkers and correlating biomarker expression to melanoma status or stage in a subject.
US20090275586 Heterocyclic inhibitors of pde4 The present invention is directed to potent and selective heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role.
US20090142394 Gastric Antacid A novel particulate composite hydrotalcite which offers antacidic effect comparable to that of a particulate hydrotalcite so far used as a gastric antacid and, further, offers excellent stomach inner wall protection effect. A particulate composite hydrotalcite represented by the following formula (1), (MgaZnb)1-xAlx(OH)2(An−)x/n ·mH2O (1) wherein An− is CO3 2−, SO4 2− or Cl−, n is 1 or 2, and x, a, b and m are values that satisfy the following conditions, 0.18≦x≦0.4, 0.5≦a<1, 0=50 to =600 mg of riboflavin, >=50 to =800 mg of magnesium and >=15 to =500 mg of coenzyme Q10, related to the daily dosage. Independent claims are also included for: (1) preparation (C1) comprising lactic acid bacteria, where the omega-3-fatty acids and/or vitamin E are contained in a capsule; and (2) a food, preferably food supplementary agent and/or agent to the supplementing balanced diet comprising (C1). - ACTIVITY : Antimigraine. No biological data given. - MECHANISM OF ACTION : None given.
EP2424494A1 Formulation of tocotrienol quinones for the treatment of ophthalmic diseases A formulation, comprising an ophthalmically effective amount of one or more tocotrienol quinones, particularly of alpha-tocotrienol quinone is disclosed. Use of a formulation comprising one or more tocotrienol quinones for the prevention, reduction, amelioration or treatment of ophthalmic disorders that are associated with a neurodegenerative or trauma disorder is also discussed. A method of treating or controlling the ocular symptoms associated with neurodegenerative diseases or trauma with a formulation comprising one or more tocotrienol quinones is also discussed. A method of treating or controlling the ocular symptoms associated with mitochondrial myopathies with a formulation comprising one or more tocotrienol quinones is also discussed.
US20050053660 Multi-particulate form of medicament, comprising at least two differently coated forms of pellet The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.
US20090227655 Nonviral vectors for delivering polynucleotides to target tissue Methods and compositions for delivering polynucleotides are provided. One embodiment provides a non-viral vector comprising a recombinant polynucleotide-binding protein comprising a protein transduction domain operably linked to a targeting signal.
WO2014020155A1 Oral transmucosal adminstration forms of s-ketamine The present invention relates to methods and compositions for the treatment of pain, in a preferred embodiment relating to the oral transmucosal administration of S-Ketamine, its salts or derivatives.
CN101210016B Heterocycle-fused morphinans compounds, preparation method and use thereof The present invention discloses an aromatic or aliphatic heterocyclic condensed morphinan compound, a synthesis method thereof, and such applications thereof as opioid receptor agonist or anti-agonist in treating drug abuse and as novel painkiller. The general structural formula of the compound is shown in (I), wherein, R is H, straight chain or branch chain alkyl of C1 to C10, aromatic group or aliphatic heterocyclic or non-heterocyclic substituted alkyl; X is H, -OH, alkoxy, amido, substituted amido, carboxyl, ester group, aminoacyl; Y is H, -OH, alkoxyl, amido, substituted amido, etc., and Z is various substituted pentagon, hexagon or substituted pentagon, hexagon aromatic and aliphatic heterocycle.
WO2010086746A3 Compositions and methods of treating viral infections The present invention relates to the field of nutraceuticals, and in particular to nutraceuticals comprising sulfated polysaccharides, Astragalus polysaccharides, resveratrol, and combinations thereof. These compositions find use in inducing physiological responses such, decreasing body fat, increasing lean body mass, alleviating the symptoms of colds, preventing the onset of colds, increasing energy, increasing the feeling of well-being in subjects, and improving skin tone and appearance.
CN101475526A Carboxylic acid derivatives inhibiting the binding of integrins to receptors thereof A method for the inhibition of the binding of alpha4beta1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and to the use of such compounds either a above, or in formulations for the control or prevention of diseases states in which alpha4beta1 is involved.
US20100317740 Method for Predicting Response to Tamoxifen This invention relates, e.g., to a method for predicting the response of a subject having, or at risk of developing, breast cancer to Tamoxifen therapy. The method comprises measuring the amount of phosphorylation at residues S70 of Bcl-2, Y992 of EGFR, and/or Y527 of Src in a suitable sample from the subject, wherein a statistically significantly elevated level of phosphorylation at one or more of the three residues compared to a baseline value indicates that the subject is likely to be responsive to Tamoxifen therapy.
US7001902 Cyclization in presence of Lawesson's reagent Compound corresponding to the general formula (I) in which R1, R2, R3, R4 and R5 each represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, trifluoroalkoxy, cyano, hydroxyl, (C1–C6)alkyl or (C1–C6)alkoxy group and R6 represents a (C1–C6)alkyl group. Therapeutic application.
US7053219 such as 5-methyl-6-(4-methoxyphenyl)-3-pyridin-4-yl-isoxazolo[4,5-c]pyridin-4(5H)one which has metabotropic glutamic acid receptor-antagonistic effect; for treatment of anxiety disorders, psychosomatic disorders, and eating disorders The invention relates to isoxazolopyridone derivatives of a formula (I-a): wherein R1a represents an optionally-substituted heteroaryl or phenyl group, R2a represents an optionally-substituted phenyl or heteroaryl group, and R3a represents a methyl group, provided that, (1) when R1a is an unsubstituted phenyl group, then R2a must not be a para-substituted phenyl group of which the substituent is any of a methoxy group, a chloro group, a methyl group, a trifluoromethyl group, a fluoro group, a bromomethyl group or a dimethylaminomethyl group, and R2a must not be an unsubstituted heteroaryl group, and (2) when R1a is a 4-tolyl group or a 4-fluorophenyl group, then R2a must not be an unsubstituted phenyl group, a 4-methoxyphenyl group or a 4-fluorophenyl group, or their pharmaceutically-acceptable salts. The isoxazolopyridone derivatives or their pharmaceutically-acceptable salts of the invention have a metabotropic glutamic acid receptor-antagonistic effect, and are useful for remedy of, for example, anxiety disorders, psychosomatic disorders, obsessive-compulsive neurosis, bipolar disorders, melancholia, eating disorders, schizophrenia, multi-infarct dementia, Alzheimer disease, epilepsy, Parkinson disease, Huntington's chorea, pain or retrograde neurosis.
WO2009136375A1 Treatment of interstitial cystitis The present invention relates to the use of (3S,5R)-3-aminomethyl-5-methyloctanoic acid, or a pharmaceutically acceptable salt or solvate thereof, for the treatment of a pain and/or a lower urinary tract symptom(s) (LUTS) associated with interstitial cystitis and/or painful bladder syndrome and/or bladder pain syndrome.
US20090142316 Use of Dendrimers to Stimulate Cell Growth The present invention relates to the use of dendrimers with monophosphonic or bisphosphonic terminations in order to stimulate the growth of cell cultures or to activate cells in culture.
US20110217315 Methods and compositions for risk prediction, diagnosis, prognosis, and treatment of pulmonary disorders The invention provides diagnostic and therapeutic targets for pulmonary disease, in particular, fibrotic lung disease. The inventors have found that a genetic variant MUC5B gene is associated with increased expression of the gene, increased risk of developing a pulmonary disease, and an improved prognosis and survival among those developing the pulmonary disease.
CN102219759A Aryl methanamide compounds and preparation method, medicinal compositions and application thereof The invention relates to the field of medicinal chemistry and medicinal therapeutics, in particular to new aryl methanamide compounds and a preparation method thereof, and also relates to application of the compounds to the preparation of medicaments for preventing or treating diabetes and metabolic syndrome diseases and medicinal compositions containing the compounds.
EP1529050B1 Cephalosporins A compound of formula (IA) or of formula (IB), wherein the substituents have various meanings, useful as a pharmaceutical.
US20110144195 Methods for synthesizing glycinols, glyceollins i and ii, compositions of selected intermediates, and therapeutic uses thereof Two distinct methods are disclosed and claimed for synthesizing glyceollin I plus glyceollin II as a mixture and as their pure forms. Stereochemical isomers and various synthetic intermediates are also synthesized and claimed for their novel compositions of matter. All compounds and their mixtures are claimed for use in formulations that are useful to treat or prevent cancer, or that have utility as selective estrogen receptor modulators, such formulations including enhanced or medical foods, dietary supplements and ethical pharmaceutical agents.
EP2545917A1 Novel ep4 agonist Provided are a compound which is superior in metabolic stability, and selectively binds to an EP4 receptor, and a medicament containing same. It has been found that a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1 - 3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1 - 4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, has, unlike known PGI2 analogs, a selective EP4 agonist action, and therefore, a medicament containing the compound is useful for the prophylaxis and/or treatment of immune diseases, cardiovascular diseases, cardiac diseases, respiratory diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, diseases of the digestive tract, neurological diseases, skin diseases and the like.
CN103585314A Hawthorn vitamin C tablet and production method thereof The invention provides a hawthorn vitamin C tablet and a production method thereof. The hawthorn vitamin C tablet is prepared by the following components by weight: 150-400 parts of hawthorn micro-powder, 50-100 parts of vitamin C, 2-8 parts of vitamin C, 13 parts of vitamin B3, 10 parts of vitamin B3, 13 parts of vitamin B5, 4-20 parts of an adhesive, and 10-30 parts of a lubricant, wherein the adhesive is hydroxypropyl methyl fiber and povidone; the lubricant is silicon dioxide. The invention further provides the production method of the hawthorn vitamin; products obtained through adopting the formula and corresponding production method have dual medical effects of hawthorn and vitamin C; at the same time, the production method overcomes difficulties when the vitamin C products are prepared; the obtained finished products have excellent quality.
CN1611509A Nucleic acid adaptor for specific identifying human cerebral acetylcholinesterase and its use The invention offers oligonucleotide adapter of specific combining human-brain acetylcholinesterase containing SEQ ID: 1, SEQ ID: 2 or SEQ ID: 3 sequence, method of detecting or discriminating human-brain acetylcholinesterase, method and diagnostic reagent and medicine to diagnose or therapy the disease relating to human-brain acetylcholinesterase (especially neural tube defect and neurotic disorder), and so on.
US20110244042 Stabilized formulations of cns compounds Formulations of molindone having superior stability and methods of administering same are provided. The formulations may be immediate, modified, or otherwise delayed release formulations of molindone.
WO2007035154A1 Novel n-pyrazinil-phenylsulfonamide derivatives as chemokine receptor modulators for use in the treatment of asthma The invention provides a compound of formula (I), wherein R1, R2 and R3 are as defined in the specification, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
CN1948305A New dioxo morpholine kind compound, its preparation method and use The present invention relates to a new dioxomorpholine compound, preparation containing said compound, its production method and application.
CN101385826B Health care medicinal liquor for strenthening yang and preparation method thereof The invention discloses health wine for tonifying yang and a preparation method thereof. By adopting the technology of pharmaceutical preparation, the wine base is blended, flavor blended and seasoned, the fleece-flower root health wine for tonifying yang in the invention is characterized by integrated wine body, moderate alcohol content, dark brownish red and clarified wine color, mellow, mild and fragrant flavor and long aftertaste, without going to the head after drunk. Being added with microelement zinc, the health wine can have more obvious, mild and lasting effect. After being proved bymore than 300 cases, the wine has such good effect according to the unanimous responses: 75% of people who drink the wine for one or two days can obtain the effect on enhancing sexual function and improving anti-fatigue capacity of the body. As the wine has the functions of invigorating the kidney and strengthening the yang, nourishing the liver and replenishing essence, strengthening the spleen and stomach, expelling wind and removing dampness and prolonging the life, the regular drinking of the wine can replenish essence and strengthen the yang, enhance the qi and blood function of the human body and activate the life vigor, thus fundamentally conditioning the functions of viscera, improving sexual functions and the sexual life quality of the middle-aged and old men.
EP2019113A1 New Crystalline Salts of 5-Amino-3-(2',3'-di-O-acetyl-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one The invention relates to new crystalline salts of 5-amino-3-(2',3'-di-O-acetyl-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one, their production and usage, and pharmaceutical preparations containing such salts and crystalline forms.
WO2014124132A1 Stable pharmaceutical composition of clopidogrel free base for oral and parenteral delivery The present disclosure provides ready-to-use, oil/water emulsion compositions with mean droplet size (intensity-average, nm) of 100-500 nm,, wherein the oil phase comprises clopidogrel free base dispersed in pharmaceutical acceptable oil(s). The emulsion uses clopidogrel free base or premix of clopidogrel free base in oil(s) as the starting materials and may also contain one or more excipients such as surfactant and or co-surfactant, osmotic agent, pH adjustment agent, antioxidant, preservative, sweetener, and/or suspending agent, etc. The emulsion formulations and method of manufacturing significantly improves the stability of clopidogrel over other aqueous based formulations (such as cyclodextrin-based formulations and emulsion made using clopidogrel salt as the starting materials) with respect to chiral degradation, hydrolytic, and thermal degradation. Ready-to-use emulsion compositions, which can be administered orally or parentally as a single high dose with up to 300 mg of clopidogrel dose, can be prepared and stored at room temperature for at least 19 weeks or at refrigeration temperature for at least 1 year. The compositions will provide rapid therapeutic action as anti¬ platelet agent for patient under emergence and intense care or who cannot swallow tablet dosage form.
CN102389426A Application of isoquinoline type alkaloids and derivatives thereof to preparation of medicine for inhibiting HPV (Human Papilloma Virus) infection The invention relates to an application of isoquinoline type alkaloids and derivatives thereof to preparation of a medicine for inhibiting HPV (Human Papilloma Virus) infection, belonging to the field of natural medicine extract preparation and anti-virus and anti-tumor officinal application. The invention provides an application of corydaline, isocorydine, isoboldine, N-methyl hernovine, dicranostigma leptopodum or pharmaceutically acceptably salts or esters to the preparation of the medicine for treating the HPV infection.
CN101386593A Norfloxacin glutamate hydrate and preparation and use thereof The invention relates to a glutamic acid norfloxacin hydrate, which is characterized in that the glutamic acid norfloxacin hydrate is C16H18FN3O3.C5H9NO4.nH2O, wherein n is equal to between 0.5 and 3.5; and the glutamic acid can be L-type, D-type or DL-type glutamic acid. The crystalline hydrate has the advantages of good water solubility and good storage stability, and is applicable to the treatment and the prevention of infectious diseases on people or animals caused by Gram-positive or negative bacterial sensitive organism.
WO2009149621A1 Use of icariside ii in manufacture of products for preventing or treating male or female sexual dysfunction The present invention provides the use of icariside II or extract comprising thereof in manufacture of products for preventing or treating male or female sexual dysfunction, in particular, the use for improving pathological or organical tissues of patients with erectile Dysfunction.
CN103380784A Bactericidal odor removing agent The invention discloses a bactericidal odor removing agent in the chemical mixture agent field, and is characterized by comprising the components, in percentage by weight: (A) 0.25 to 5% of an organic silicon quaternary ammonium salt; (B) 0.1 to 2% of an organic silicon coupling agent; (C) 0.2 to 2% of a stabilizing agent; and (D) the balance being deionized water. The bactericidal odor removing agent has antibacterial, mildewproof, odor-removing and deodorant effects, has lastingly bacteriostatic effect and widely bacteriostatic range, simultaneously is safe and reliable for any product, and does not pollute the environment. The organic silicon quaternary ammonium salt has bactericidal and bacteriostatic effects, and non-toxic, gentle, soft and smooth properties of the organic silicon quaternary ammonium salt to human bodies are utilized, so the bactericidal odor removing agent is prepared into a spray medicament form, is used for disinfectant and bactericidal treatment of various traumatic infections and skin infections, can have rapidly bactericidal antipruritic effect for the various skin infections, and can kill bacteria and inhibit bacterial activity.
WO2009057768A1 Anti-fungal agent and anti-bacterial agent The object is to provide: an antimicrobial agent against Listeria monocytogenes, which has been believed to be a causative bacterium for listeriosis, an acidophilic bacterium such as Alicyclobacillus acidoterrestris, and a mold; and an anti-bacterial agent having a more potent anti-bacterial effect against a broader range of bacteria compared with conventional anti-bacterial agents. An antimicrobial agent having an antimicrobial effect against Listeria monocytogenes, an acidophilic bacterium and a mold can be provided by using lysophosphatidylglycerol as an active ingredient. An anti-bacterial agent having a potent anti-bacterial effect against a broader range of bacteria can be provided by using lysophosphatidylglycerol in combination with a conventional anti-bacterial agent.
CA2590223C Oral compositions containing extracts of rosmarinus and related methods Addition of rosemary extract to various dentifrice compositions results in tooth paste, mouth rinses, and other compositions that are suitable for treating and preventing a variety of oral disease including gingivitis, plaque build-up, and the like. Rosemary extract, containing major amounts or ursolic acid and carnosic acid, is added to dentifrice compositions so that the amount delivered to the oral cavity upon use is effective to provide an antibacterial, antioxidant, and/or anti-inflammatory effect. In various embodiments, the components of rosemary extract are combined with triclosan or other phenolic antibacterial agents to provide enhanced activity.
US7138543 Thiolalkyl benzoic acid derivatives The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-β activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.
WO2014139681A1 Crystalline cis-(e)-4-(3-fluorophenyl)-2',3',4',9'-tetrahydro-n,n-dimethyl-2'-(1-oxo-3-phenyl-2-propenyl)-spiro[cyclohexane-1,1'[1h]-pyrido[3,4-b]indol]-4-amine The present invention relates to crystalline forms of cis-(E)-4-(3-Fluorophenyl)-2',3',4',9'- tetrahydro-N,N-dimethyl-2'-(1-oxo-3-phenyl-2-propenyl)-spiro[cyclohexane-1, 1 '[1 H]- pyrido[3,4-b]indol]-4-amine, pharmaceutical compositions and medicaments comprising these modifications, the use of these modifications as well as to a process for making the crystalline forms.
CN102048791A Method for preparing sinigrin extract The invention discloses a method for preparing a sinigrin extract. The method comprises the following steps of: 1) extracting crucifer brassica mustard leaf, cabbage or broccoli serving as a raw material by using acetic acid, and centrifuging the extract to obtain supernate; 2) adding ethanol into the supernate, adjusting the ethanol concentration to be 80 to 85 percent, standing the solution for 1 to 1.5 hours, centrifuging the solution, and collecting secondary centrifugate; 3) concentrating the secondary centrifugate till no ethanol smell, filtering the concentrated centrifugate by using a ceramic film of 0.5 micron, concentrating the permeating solution until the volume of the permeating solution is 2 to 3 times weight of the raw materials to obtain concentrated permeating solution; and 4) filling the concentrated permeating solution into a macroporous resin column, collecting the effluent, eluting the effluent by using water in an amount which is 2 to 3 times weight of the resin, collecting eluant, combining the effluent and the eluant, and performing concentration and freeze drying to obtain the sinigrin extract. The method has simple process and is easy to operate, the sinigrin content of the obtained product can reach 20 to 40 percent, and the extraction rate of the sinigrin reaches over 80 percent.
WO2011044499A2 Enterotoxigenic e. coli fusion protein vaccines The disclosure relates to fusions of enterotoxigenic Escherichia coli (ETEC) polynucleotides and polypeptides. In one example, a toxiod heat-labile (LT) and heat-stable (STa) fusion is described. This fusion may include LT with a substituted amino acid at position (192), a linker, and STa with a substituted amino acid at positions (11, 12, 13, or 14). Further provided are vaccines containing the disclosed fusions. Example methods for administering to a subject the disclosed vaccines and using the fusions and vaccines to reduce or eliminate contamination of a food or water supply are additionally contemplated.
WO2014120994A1 Rufinamide and derivatives and their use in modulating the gating process of human voltage-gated sodium channels The present invention provides compounds of formula I or a salt, solvate, or stereoisomer thereof, wherein X is H, or an electron withdrawing group such as a halogen, NH2, NO2, SO2, CN, or a C1-C6 alkyl group; Alk is C1-C3 alkyl; R1 is H, C1-C6 alkyl, which may be substituted with OH, NH2, acyl, sulfonyl, and cyano groups; and R2, is C1-C6 alkyl, which may be substituted with OH, NH2, acyl, sulfonyl, and cyano groups. Pharmaceutical compositions comprising these compounds and/or rufinamide are also provided. Methods for prevention and treatment of epilepsy disorders such as Lennox-Gastaut Syndrome (LGS), and modulation of voltage-gated sodium (Nav) channels are Nav1.1 channels by administration of these compounds and/ or rufinamide are also provided.
US20120157425 New compounds, pharmaceutical compositions and uses thereof The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
US20120010176 Utrophin promoter activity upregulation for the treatment of muscular dystrophy Methods are provided for increasing utrophin promoter activity, utrophin expression or utrophin activity, and treating or reducing the symptoms of muscular dystrophy by administering to a subject in need thereof an effective amount of a composition comprising a utrophin promoter or activity upregulator. Muscular dystrophy includes but is not limited to Duchenne muscular dystrophy, Becker's muscular dystrophy, limb girdle muscular dystrophy, or a disease characterized by mutation or dysregulation of the dystrophin gene or an aberrant or dysfunctional dystrophin.
EP2575765A2 Oral spray formulations and methods for administration of sildenafil The present disclosure is directed to chemically-stable and pharmaceutically- acceptable sildenafil oral spray formulations for the treatment of male erectile dysfunction, wherein the oral spray formulation has a pH of about 1.5 to less than 3.0. The present disclosure is also directed to methods for treating male erectile dysfunction.
US7319101 catechol-O-methyltransferase (COMT) inhibitors such as N-{3-[5-(6-Amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-yl]-allyl}-2,3-dihydroxy-benzamide used for the treatment of schizophrenia, Parkinson's disease and as antidepressants or cognition activators The present invention relates to compounds of formula I wherein R1 is as defined in the specification and to esters thereof which are hydrolyzable under physiological conditions and to the pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of COMT and, thus, are useful for the treatment of diseases for which COMT inhibition is beneficial. The invention further relates to the treatment, control, or prevention of diseases such as depression, schizophrenia, Parkinson's disease, and to improve cognition.
EP1915350A1 Amide derivatives The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen and R4 is , (1-6C)alkyl or (1-6C)alkoxy; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
US20080146540 Identifying genetically at risk persons having MAP3K9 associated presence; kits; assay techniques; treating with mixed lineage kinase inhibitors Methods for diagnosis of asthma or allergic rhinitis or a susceptibility to asthma or allergic rhinitis based on detection of at-risk haplotypes associated with MAP3K9 are disclosed. Also methods for treatment of asthma or allergic rhinitis or a susceptibility to asthma or allergic rhinitis based on detection of at-risk haplotypes associated with MAP3K9 are disclosed. In particular, pathways targeting for treating individuals who are at-risk of developing asmtha or allergic rhinitis are described. In certain aspects, MLK1 inhibitors are used in treatment methods.
WO2009053716A1 Purine derivatives useful as pi3 kinase inhibitors This invention provides a compound which is a purine of formula (Ia) or (Ib): and the pharmaceutically acceptable salts thereof that are inhibitors of PI3K and a selective for the p110δ isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arisi from abnormal cell growth, function or behaviour associated with PI3 kinase such as cance immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
US20120115848 Inhibitors of Polo-Like Kinase The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, U1, U2, U3, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
CN1976694A Topical formulations for treating allergic diseases Methods for topically treating allergic diseases of the eye, ear or nose using tricyclic compounds are disclosed.
US7141564 are active against a wide range of organisms including both Gram-negative and Gram-positive organisms Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
CN103120712A Nanoemulsion spray for inflammation reducing and pain easing of wounds and preparation method of nanoemulsion spray The invention discloses nanoemulsion spray for inflammation reducing and pain easing of wounds. Nanoemulsion has grain diameter of 1-100nm and is composed of 30-45% of surfactant, 0.5-5% of cosurfactant, 1-5% of olibanum oil, 1-5% of myrrh oil, 1-2% of angelica oil, 1-3% of notopterygium oil, 1-5% of opoponax oil, 0.1-1% of paeonol, 0.5-2.5% of azone and balance deionized water. The nanoemulsion spray is specific drug for external use and has multiple functions of sterilization, inflammation reducing, deflating, pain reliving, putridity eliminating and muscle engendering, wound-healing promoting and the like. Transdermal absorption rate of each active ingredient in a compound is increased, and the nanoemulsion spray can be directly sprayed to wound surfaces, is needless of debridement, free of clothes pollution, good in astringing and muscle-engendering effect and free of scars, and has new efficacies on eliminating, pus drawing and necrotic tissue removing for skin and external diseases.
US20080275121 For contact lenses; surface treatment The present invention relates to methods for disinfecting or cleaning a contact lens comprising contacting a contact lens with a formulation comprising a N-halogenated amino acid and a phase transfer agent for a time sufficient to disinfect or clean the lens. This specification further discloses a formulation for disinfecting a contact lens comprising an N-halogenated amino acid and a phase transfer agent.
US20090093513 Method to Use Compositions Having Antidepressant Anxiolytic and Other Neurological Activity and Compositions of Matter The sponges were collected from a variety of locations in the Florida Keys and separated based on morphology and color. The samples were identified as three species, two of which are well known: V. rigida (Esper, 1794) (order Verongida, family Aplysinidae) and S. aurea (Hyatt, 1875) (order Dictyoceratida, family Thorectidae), and a third S. cerebriformis (Duchassaing & Michelotti, 1864), is less common and separated based on subtle differences of morphology and coloration, from the other two species. Several compounds were isolated and were evaluated in established animal models predictive of neurological related drug function, namely, the rodent FST and the chick anxiety-depression model.
CN102048718A Medical application of enamine ketone compound The invention relates to the medical application of an enamine ketone compound, in particular to the medical application of a chemical formula (I, II and III) substituted enamine ketone compound and a compound preparation thereof to the treatment of nervous system disorder. The compound and the compound preparation are mainly used for treating and/or preventing anxiety disorder, depression, mania, epilepsia, and neuron injury and neuralgia which are caused by various factors. The invention also relates to the preparation of the compound and the compound preparation which serve as medicaments.
CN103285400A Acid sensitive polymer prodrug, nanoparticles of prodrug and application of nanoparticles The invention discloses an acid sensitive polymer prodrug, nanoparticles of the prodrug and application of the nanoparticles. In the acid sensitive polymer prodrug, a polymer precursor is a vinyl ether-functionalized water-soluble A-B type two-block polymer; drug molecules are linked with the A-B type two-block polymer through an acetal bond; the acid sensitive polymer prodrug is self-assembled in water solution to form predrug micellar nanoparticles in which a polyethylene glycol hydrophilic chain segment serves as an outer surface and an anti-cancer drug bound to a polymer main chain through the acetal bond serves as a hydrophobic core. The pH sensitive prodrug and the nanoparticles of he prodrug are simple in preparation method, and good in tumor inhibitory effect; the nanoparticles also can efficiently encapsulate another hydrophobic anticancer drug; the kill capability to the cancer cell is enhanced; and the efficiency of endocytosis of the cell to the nanoparticles can be enhanced by coupling specific target molecules onto the surfaces of the nanoparticles. Thus, the inhibitory effect on the tumor cell is enhanced.
WO2009025239A1 Novel preparation for external use A compound represented by the general formula (I), a salt of the compound, or a hydrate of either thereof. They have an excellent antipruritic effect and have an excellent metabolic effect. The compound represented by the general formula (I), salt of the compound, or hydrate of either thereof, in a preparation for external use, has excellent absorbability into the skin. The preparation for external use has excellent stability because the ingredients incorporated are less apt to separate out even in long-term storage. (I) [In the formula, R represents hydroxy, C1-6 alkoxy optionally substituted by C1-6 alkoxy, or amino optionally substituted by C1-6 alkyl.]
CN102085214A Low-molecular citrus pectin capable of being combined with clinical common chemotherapeutic drug for controlling cancer and cancer metastasis and diffusion The invention relates to a new application of a low-molecular citrus pectin, in particular to an application of a low-molecular citrus pectin for preparing drugs, foods or health products. The drugs, foods or health products are used for being combined with a clinical common chemotherapeutic drug for controlling cancer and cancer metastasis and diffusion. The low-molecular citrus pectin and the clinical common chemotherapeutic drug are combined for controlling cancer and cancer metastasis and diffusion, wherein the cancer is colon cancer, liver cancer or cervical cancer; and the clinical common chemotherapeutic drug is PAC-1, cyclophosphamide or adriamycin.
US20070259914 Novel Piperidine Derivates as Modulators of Chemokine Receptor Ccr5. Compounds of formula (I) compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
CN102000012A Formula of mask for whitening and lightening spots The invention relates to a formula of mask for whitening and lightening spots. The mask consists of the following dry-powder materials: 10g of dahurian angelica root, 10g of white paeony root, 10g of white thistle, 10g of giant typhonium rhizome, 10g of white muscardine silkworm, 10g of white poria, 10g of bletilla, 10g of largehead atractylodes rhizome, 20g of white coix seed and 10g of lithargite. The mask has effects of nursing and treating chloasma, sunburn, freckles and radiation spots caused by dry skin, pigment rebound after peeling and pigmentation.
WO2014142221A1 Drug for respiratory diseases Provided is a therapeutic and/or prophylactic agent for respiratory diseases, or a therapeutic and/or prophylactic agent for sodium channel-mediated diseases. A pharmaceutical agent which contains, as an active ingredient, a compound represented by formula (I) or a pharmacologically acceptable salt thereof. In formula (I), each of Ar1 and Ar2 represents a heteroaryl group or an aryl group; each of R1, R2 and R3 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a cyano group; each of R4 and R5 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group; and n represents an integer of 1-3. In this connection, the heteroaryl group and the aryl group may have one or two groups that are independently selected from among a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group, a carboxyl group, a cyano group, an amino group, a C1-C3 alkylamino group and a di C1-C3 alkylamino group, and in cases where two groups are contained therein, the groups may be the same as or different from each other.
CN102796254A Pegylated celastrol and preparation method and application thereof The invention belongs to the technical field of medicine, and relates to pegylated celastrol and a preparation method and application thereof. The pegylated celastrol has a structure shown as a general formula in the specifications. The invention also provides application of the pegylated celastrol and methoxy amino polyethylene glycol 10kDa mono-modified celastrol (mPEG10k-NHCO-celastrol) to preparation of medicines for treating various malignant tumors such as prostatic cancer, lung cancer, liver cancer and cervical cancer. Celastrol is subjected to chemical structural modification by PEG, so that the problem that the celastrol has low solubility can be solved; and an injection can be prepared after the celastrol is modified by the PEG, so that the elimination half life of the celastrol can be prolonged through in-vivo injection, the toxic and side effects of the celastrol are reduced, and the administration frequency of a patient is reduced.
US20080108654 Protein kinase inhibitors; antitumor agents; such as 5-methyl-1-quinol-4-ylmethyl-3-(4-trifluoromethanesulfonylphenyl)imidazolidine-2,4-dione trifluoroacetate The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
EP2734503A1 Quinolinyl glucagon receptor modulators The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
CN102666540A Condensed azine-derivatives for the treatment of diseases related to the acetylcholine receptor The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by nicotinic acetylcholine receptors, such as schizophrenia and Alzheimer's disease.
CN101422461A Preparation method of matrine vagina effervescence tablet and use thereof The invention discloses a preparation method of a vagina effervescent tablet containing matrine, and application thereof. The invention belongs to the new technical field of medicaments and relates to a new preparation formulation of the matrine, which is used for curing colpitis, chronic cervicitis and cervical erosion caused by various bacteria and preventing and treating cervical carcinoma; moreover, the new preparation formulation can also be used as the medicament preparations of senile vaginitis and pelvic inflammation and used in the preparation methods thereof. The new preparation formulation is characterized in that after the effervescent tablet is dissolved, the pH value of the liquid thereof is between 2.5 and 5.5 and the best PH value is between 3.8 and 4.2 which approach the physiological environments of human bodies.
US7241795 2,5-bis ((alkyl (or aryl) imino) aminophenyl) furans, thiophenes or pyrroles; Mycobacterium tuberculosis, Trypanosoma spp., Candida albicans, Aspergillus spp., Cryptosporidium parvum, Giardia lamblia, Plasmodium spp., Pneumocystis carinii, Toxoplasma gondii, Fusarium solani, and Cryptococcus neoformans The present invention relates to novel 2,5-bis{[alkyl (or aryl) imino]aminophenyl}furans and thiophenes of the general formula in which R1, R2, R3 and R4 are each independently selected from the group consisting of H, alkyl, alkoxy, halide, and alkylhalide groups; R5 is H, alkyl or aryl; R6 is H, alkyl, aryl, or NR7R8, in which R7 and R8 are each independently selected from the group consisting of H, alkyl and aryl; and X is O, S or NR9, in which R9 is H or alkyl, and to the use of such compounds.
CN1931152A Application of shikonin in preparing medicine for inducing apoptosis The present invention provides the application of shikonin in preparing medicine for inducing apoptosis. Shikonin has the molecular formula of C16H16O5 and the chemical name of (+)-5, 8-dihydroxy-2-(1-hydroxy-4-methyl-3-pentenyl)-1, 4-naphthoquinone, possesses optical activity, and constitutes one pair of antimers together with isoshikonin. The present invention has clinical application foreground owing to that shikonin can kill several kinds of drug resisting tumor cells in the effect higher than other available clinical medicines and possesses relatively low toxicity.
WO2009009171A2 Methods for preventing or treating infectious diseases using gallium compounds The present invention relates to methods for preventing or treating infectious diseases caused by extracellular microorganisms, such as bacteria and fungi, by systemically administering to a patient a compound containing gallium. The extracellular microorganisms targeted by the present methods include methicillin- resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), E. coli O157:H7, fluoroquinolone-resistant Salmonella typhi, and the like. Furthermore, in the present methods, gallium compounds can be co-administered with one or more conventional antimicrobial agents to treat infectious diseases with reduced risks of creating multi-drug resistant pathogens. The methods of the present invention is also applicable to those microorganisms, such as ulcer-causing Helicobacter pylori, complete eradication of which so far has been difficult to achieve.
US20100130474 Alpha7 nicotinic acetylcholine receptor inhibitors The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory systems.
EP1792913A1 Novel secreted and membrane-associated proteins and uses therefor Novel secreted and membrane-associated polypeptides, proteins, and nucleic acid molecules are disclosed (e.g., BDSF and STMST molecules). In addition to isolated, full-length proteins, the invention further provides isolated fusion proteins, antigenic peptides and antibodies. The invention also provides nucleic acid molecules, recombinant expression vectors containing a nucleic acid molecule of the invention, host cells into which the expression vectors have been introduced and non-human transgenic animals in which a BDSF or STMST gene has been introduced or disrupted. Diagnostic, screening and therapeutic methods utilizing compositions of the invention are also provided.
US7704516 Administration be done percutaneously (topically), to avoid the first-pass effect and related liver metabolism of the 4-hydroxy tamoxifen; side effect reduction Pharmaceutical compositions of 4-hydroxy tamoxifen, particularly compositions suitable for percutaneous administration, are useful in methods for treating and preventing breast cancer. When percutaneously administered to a patient's breasts, 4-hydroxy tamoxifen concentrates locally, and exerts an anti-estrogenic effect. In patients with breast cancer, this effect reduces tumor tissue proliferation. In patients at risk for developing breast cancer, the anti-estrogenic effect prevents breast tumor formation.
EP1173757B1 Diagnosis of human kidney diseases Kidney disease is diagnosed by measuring urinary catalytic iron in humans. Progressive kidney disease is treated by administering an iron chelator to humans. In particular, the progression of kidney disease essentially can be halted and the severity of kidney disease can be reduced by the administration of iron chelators to humans afflicted with a progressive kidney disease. The methods include measuring catalytic iron content in urine in a human afflicted with a progressive kidney disease and administering an iron chelator to the human. The method can include measuring total urinary protein content, blood urea nitrogen or creatinine in a blood sample before, during or after the administration of an iron chelator.
US20090017019 Methods and compositions for modulating bmp-10 activity Methods and compositions for modulating cardiac, renal and vascular cell function and homeostasis using agonists and antagonists of BMP-10 are disclosed. In particular, methods for treating, preventing and/or diagnosing BMP-10-associated vascular, renal, fibrotic and cardiac conditions and/or disorders are disclosed. Screening methods for evaluating BMP-10 modulators, e.g., agonists and antagonists, are also disclosed.
CN1660154A Extractive and its application in medicine An extract for preventing and treating depression is extracted from 4 Chinese-medicinal materials including inula flower, hematite, bamboo leaf, etc.
CN101361737B Use of 4-tetrahydrothiazole dione derivates The invention relates to the application of 5-benzylidene-2, 4-Thiazolidinedione derivative and belongs to the field of chemical medicines. The 5-benzylidene-2, 4-Thiazolidinedione derivative has the structure as shown in formula I, wherein, R1 is hydrogen, halogeno-group, hydroxyl or alkoxy; R2 is hydrogen, halogeno-group, hydroxyl or alkoxy. Proved by experiments, the 5-benzylidene-2, 4-Thiazolidinedione derivative shown in formula I has excellent effects on curing hepatitis, colonitis, immunity myocarditis, pancreatitis and pulmonary fibrosis and other autoimmune diseases, thus providing anew choice for preparing the similar drugs.
US7723366 Cardiovascular disorders; antidiabetic agents; anticancer agents The present invention relates to methods of treatment of certain metabolic diseases, and to the use of compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, the invention relates to the use of compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the following formulae: (I) and (II) Wherein Y, C, R1, R2, R6, and R7 are defined herein.
CN103087031A Application of bistetrahydrobenzopyrone dimer compounds in anti-cancer drugs The invention belongs to the technical field of medicine, and relates to an application of a compound 1 and a compound 2 in anti-cancer drugs, wherein the compound 1 and the compound 2 are derived from a special environmental microorganism, and have tumor growth inhibition activities. According to the present invention, the compound 1 and the compound 2 have a structure formula represented by the following figure (I), have stable structure, and can be prepared into various clinically acceptable formulations after matching with appropriate pharmaceutical excipients; in vitro human tumor cell growth inhibition activity test results of the compound 1 and the compound 2 show that the compound 1 and the compound 2 provide tumor growth inhibition activity similar to a positive control drug doxorubicin, and in vivo tumor growth inhibition activity test results show that the compound 2 has characteristics of low toxicity and high tumor growth inhibition rate, and is a novel efficient and low toxicity tumor growth inhibitor; advantages of strong activity, low dosage and the like are provided; and the compound 1 and the compound 2 derived from the special environmental microorganism secondary metabolite can be used for anti-cancer drug preparation.
CN102429866A Preparation formula of ibuprofen oral solution capable of being prepared into frozen form for taking The invention relates to a preparation method of an ibuprofen oral solution capable of being prepared into a frozen form for taking. A formula comprises 0.2-4.0 percent (g/L) of ibuprofen serving as a main medicament, 1.0-40.0 percent (g/L) of hydroxypropyl-beta-cyclodextrin and 50.0-98.0 percent (g/L) of water. The oral solution prepared according to the formula can be taken by a patient in an oral solution way, and can be frozen to the condensed state in the refrigerator refrigerating environment (at the set temperature of 0 DEG C to 20 DEG C below zero) used in an ordinary household for taking. According to the formula, the aim of enhancing the administration adaptability of a patient, particularly a child patient, is fulfilled.
WO2007024611A3 Sulfonamides of 7 -aminoheptanoic acid derivatives for treating glaucoma The present invention provides wherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5; R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH; R3 is selected from the group consisting of C1C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl; R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl; m is 0 or an integer from 1 to 3 and n is an integer of from 1 to 4. These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.
US20100099752 Pharmaceutical composition containing bicyclic type compounds The present invention relates to pharmaceutical compositions containing bicyclic type compounds and to methods of using same, for example, in the treatment or prevention of anxiety, mania, depression, disorders associated with a subarachnoid haemorrhage or neural shock, the effects associated with withdrawal from substances of abuse, Parkinson's Disease, psychosis, migraine and/or cerebral ischaemia.
US20100004284 Novel Heterocyclic Compounds as Positive Allosteric Modulators of Metabotropic Glutamate Receptors The present invention relates to new compounds which are Heterocyclic derivatives of formula (I) wherein A, B, P, X, Y, Q, W, R1 and R2 are defined in the description. Invention compounds are useful for treating central or peripheral nervous system disorders and other disorders which are affected by the neuromodulatory effect of mGluR5 positive allosteric modulators such as cognitive decline and also to treat both positive and negative symptoms in schizophrenia.
WO2011125245A1 Method for prediction of prognosis of small cell lung cancer, method for treatment of small cell lung cancer, method for amelioration of prognosis of small cell lung cancer, and method for screening for therapeutic agent for small cell lung cancer, each utilizing mirna Disclosed are a method for predicting the prognosis of small cell lung cancer, a method for treating small cell lung cancer, a method for ameliorating the prognosis of small cell lung cancer, a therapeutic agent for small cell lung cancer, and a method for screening for a therapeutic agent for small cell lung cancer, each of which utilizes miRNA. Specifically disclosed are: a method for diagnosing the prognosis of a small cell lung cancer patient, which employs miR-153, miR-196a, miR-203 or miR-216a as a measure; a method for ameliorating the prognosis of small cell lung cancer, which employs the above-mentioned substance as a measure; a method for treating small cell lung cancer, which targets the above-mentioned substance; a therapeutic agent for small cell lung cancer; and a method for screening for a therapeutic agent for small cell lung cancer, which utilizes the above-mentioned substance.
WO2006053109A1 Heteroaryl compounds This invention relates to compounds of formula (I) their compositions and methods of use thereof. The compounds (and compositions) are useful in modulating IL-12 production and processes mediated by IL-12.
CN101525316A Quinoline derivatives, preparation method and applications thereof The invention relates to new substituted quinoline derivatives presented in general formula (1a), or general formula (1b) or general formula (1c), a medical acid added salt, a stereochemical heterogeneous formula and a tautomeric form thereof. The compound can be used for curing mycobacterium diseases, in particular to diseases caused by pathogenic mycobacteria, such as mycobacterium tuberculosis, mycobacterium bovis, mycobacterium avium and mycobacterium marinum and is particularly defined as following: R1 is mutually independent bromines; p is equal to 1, R2 is an alkoxy, and R3 is a randomly substituted phenyl or naphthyl; q is equal to 1, R4 and R5 are mutually independent hydrogen and a methyl or an ethyl, and R6 is hydrogen; r is equal to 0 or 1 and R7 is hydrogen. The invention also relates to a composition of the compound, applications of the compound of the composition to medicines for curing the mycobacterium diseases, and a method for preparing the compound of the composition, which comprises a medical carrier and is used as activated ingredient of curable effective quantity.
US20080255106 N-(3-Methoxypropyl)-2-[2-(trifluoromethyl)phenyl]-3H-imidazo[4,5-b]pyridine-7-carboxamide hydrochloride; antidepressant, analgesic, anxiolytic agent; amyotrophic lateral sclerosis, Down syndrome, Huntington's Disease, bipolar disease, affective disorders, depression, schizophrenia, cognitive disorder Compounds of formula I wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation and new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
CN102846643A Application of salidroside in treating C-type fanconi anemia The invention discloses application of a compound of salidroside in preparing pharmaceuticals for treating C-type fanconi anemia. The compound has stronger promotion effects on hematopoietic colony formation, can be used for developing the pharmaceuticals for treating C-type fanconi anemia, meets the clinical demands, and has excellent market value.
US7312358 Dysmenorrhea; congestive heart failure; liver disorders; vision defects The present invention relates to sulfanilide derivatives of formula (I), in which R1 and R2 are optionally substituted aryl and heteroaryl groups and the other variables are as defined in the claims, for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such sulfanilide derivatives. Said derivatives are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to sulfanilide derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin, including preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. The present invention is furthermore related to novel sulfanilide derivatives as well as to methods of their preparation.
EP1347778B1 Behavior chemotherapy A protocol for permanent modification of behavior and elimination of undesired habits is described. The protocol involves stimulating the implicit memory, followed by continuing such stimulation in conjunction with psychological treatments followed by continuing said stimulation of the implicit memory and, in addition, stimulating the explicit memory. Use of this protocol results in a permanent replacement of undesirable behaviors with desirable ones.
WO2007010044A1 3-indolylmethylene derivatives with cytostatic action The invention relates to 3-indolylmethylene derivatives having the general formula I with cytostatic action, and to a process for preparing the 3-indolylmethylene derivatives, to their use for producing medicaments, and to pharmaceutical compositions comprising 3-indolylmethylene derivatives.
CN101267821B Use of FLT3 inhibitor and a farnesyl transferase inhibitor in preparing medicine for synergistic modulation of FLT3 kinase The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from alkylquinoline and alkylquinazoline compounds of Formula (I'). Included within the present invention is both prophylactic andtherapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
US20110201653 Method for inhibiting and/or preventing formation of cancer metastases and secondary malignant cancer The invention relates to a method for inhibiting and/or preventing formation of cancer metastases and secondary malignant cancers by administration to a subject of an effective amount of a quaternary pyridinium salt of formula I wherein R′ is selected from the group consisting of H, OH, CONH2, COCH3, R″ is selected from the group consisting of H, CH3, R′″ represents H or CH3, and X− is a pharmaceutically acceptable counterion.
EP1485090B1 Combinations comprising an epothilone derivative and an imidazotetrazinone The invention relates to a pharmaceutical combination which comprises (a) an alkylating agent and (b) an epothilone derivative of formula (I) wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl, and Z is O or a bond. Said combination can be useful for the treatment of a proliferative disease, especially a tumor disease.
CN103006694A Recipe of rehydration salt for curing various animal hypertonic dehydration and preparation method of rehydration salt The invention discloses a recipe of rehydration salt for curing hypertonic dehydration of various animals and a preparation method of the rehydration salt. The recipe comprises the following materials: 5.1 g of sodium chloride, 0.2 g of potassium chloride, 0.4 g of glucose and 1.9 g of sodium lactate. During use, each 0.77 g of the rehydration salt is dissolved in 100 ml of distilled water; and a user can drink freely. The recipe is an optimal recipe for rehydration of hypertonic dehydration cases; the preparation method is simple and convenient to operate; and suitability for popularization and application is obtained.
EP1824863A1 Silicon compounds and their use A compound of any of formulas (I) to (V) : wherein at least one of Y and Z includes a Si atom, is of utility in therapy.
CN102488906A Superparamagnetic electric conductive gamma-iron oxide/polyaniline-lonidamine (gamma-Fe2O3/PAn-Lon) and preparation method thereof The invention relates to superparamagnetic electric conductive gamma-iron oxide/polyaniline-lonidamine (gamma-Fe2O3/PAn-Lon) and a preparation method thereof. The method comprises the following steps of: mixing aniline and a hydrochloric acid solution to obtain a mixed solution which contains sodium dodecyl benzene sulfonate, adding gamma-Fe2O3, stirring, and adding ammonium persulfate, wherein the molar ratio of the ammonium persulfate to the aniline is 1:1; reducing by using ammonia water to obtain eigen polyaniline, washing by using water, and drying in vacuum to obtain gamma-Fe2O3/PAn; and adding the gamma-Fe2O3/PAn into a Lon acidic solution, stirring, performing suction filtering by using a vacuum pump, washing by using water, and drying in vacuum to obtain the gamma-Fe2O3/PAn-Lon. The defects that the treatment effect cannot be limited in the specific cancerous cell, tissue or organ and normal tissue is damaged are overcome; and by the gamma-Fe2O3/PAn-Lon, the treatment effect can be limited in the specific cancerous cell, tissue or organ, the normal tissue is not damaged, and the specific pathological cell is identified through electric conductivity of an organism in an organism microenvironment, so that the Lon can better enter a lesion site, and the toxic and side effects of the Lon on healthy tissue are reduced.
WO2008120004A1 Combination of a mek- inhibitor and a b-raf inhibitor for the treatment of cancer This invention relates to a combination product comprising a MEK inhibitor and a B-raf inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to: a combination product comprising a MEK inhibitor and a B raf inhibitor; a combination product comprising a kit of parts comprising a MEK inhibitor and a B-raf inhibitor; use of the combination product in the treatment of cancer; a method of treating cancer comprising administering the combination product to a patient. The combination product and methods of the invention are also useful in the treatment of other diseases associated with the activity of MEK, and/or B-raf.
US20110224303 Use of ci-994 and dinaline for the treatment of memory/cognition and anxiety disorders The invention relates to methods and compositions for promoting cognitive function and/or treating cognitive function disorders and impairments. In particular the methods are accomplished by administering to a subject CI-994 or dinaline or a pharmaceutically acceptable salt, ester, prodrug or metabolite thereof.
US8759006 PSCA: prostate stem cell antigen and distinguishing androgen receptor negative prostate cancer from benign prostatic hyperplasia The invention provides a novel prostate cell-surface antigen, designated Prostate Stem Cell Antigen (PSCA), which is widely over-expressed across all stages of prostate cancer, including high grade prostatic intraepithelial neoplasia (PIN), androgen-dependent and androgen-independent prostate tumors.
WO2012117334A8 Mglur5 positive allosteric modulators for use in the treatment of phelan-mcdermid syndrome The invention concerns a novel therapeutic application for positive allosteric modulators of the metabotropic glutamate receptor mGluR5, notably for the therapeutic treatment of Phelan-McDermid syndrome caused by 22qI3 deletion. For this purpose, a preferred positive allosteric modulator is 3-cyano-N-(1,3-diphenyl-1-H-pyrazol-5-yl)benzamide, abbreviated as CDPPB.
CN101161247A Potassium muriate stomach-inner retention floationg type slow release tablet prepared with shuck powder as carrier The present invention is with oyster shuck powder as carrier to prepare potassium chloride stomach retention floating type slow release tablet, belonging to pharmaceutical preparation technique field. The technique is characterized in that its main components are oyster shuck powder and potassium chloride. The tablet can retain in stomach and prolong the medicine releasing time, improve the medicine absorption, be beneficial to promote bioavialability. The preparing technique process of the present invention is simple, convenient and reasonable operation, suitable for industrial production. And the price is achievement, using convenient, beneficial to large scale spreading and application. The medicine has calcium-replenishing function while treating hypokalemia, and relieved toxic effect of potassium ion to heart. The present invention has little dosage, good effect, and good market prospect.
EP1832663A2 Uses of DNA-PK This invention provides a method for increasing the susceptibility of a cell to DNA-damaging agents, comprising introducing into the cell an antisense oligonucleotide that specifically hybridizes to a nucleic acid encoding a DNA dependent protein kinase subunit so as to prevent expression of the DNA dependent protein kinase subunit; wherein the antisense oligonucleotide is in an amount sufficient to increase the sensitivity of the cell to heat, chemical, or radiation-induced DNA damage; and wherein the DNA dependent protein kinase subunit is a DNA dependent protein kinase catalytic subunit, a Ku70, or a Ku80. This invention also provides a method of treating a tumor in a subject, comprising administering to the subject an antisense oligonucleotide that specifically hybridizes to a nucleic acid encoding a DNA dependent protein kinase subunit so as to prevent expression of the DNA dependent protein kinase subunit; wherein the antisense oligonucleotide is in an amount sufficient to increase the sensitivity of the tumor to heat, chemical or radiation-induced DNA damage; and wherein the DNA dependent protein kinase subunit is a DNA dependent protein kinase catalytic subunit, a Ku70, or a Ku80. This invention provides an antisense oligonucleotide that specifically hybridizes to a nucleic acid encoding a DNA dependent protein kinase subunit, wherein the DNA dependent protein kinase subunit is a DNA dependent protein kinase catalytic subunit, Ku70, or Ku80, so as to prevent expression of the DNA dependent protein kinase subunit.
CN101229259A External salve for treating pustule The invention relates to a production method and a proportion of an ointment, in particular to an externally-used salve used for treating pus; the invention provides the ointment with synthesized efficacy and low cost. The externally-used salve used for curing pus has the following ingredients which are counted by proportioning by weight: sophora flavescens of 30 to 60g, rhizoma coptidis of 10 to 30g, phellodendron of 20 to 40g, calcined alum of 10 to 20g, bitter almond of 10 to 30g, baikal skullcap root of 10 to 30g and balsam. The optimal weight percentage of the input medicine is as following: sophora flavescens of 45g, rhizoma coptidis of 20g, phellodendron of 30g, calcined alum of 15g, bitter almond of 20g, baikal skullcap root of 20g and balsam. The ingredients power is sieve for 100 meshes and is stirred into paste with balsam. After adopting such mixture ratio and owing to adopting sophora flavescens, rhizoma coptidis, phellodendron, calcined alum, bitter almond, baikal skullcap root and balsam, the invention has the medicine effects of detumescence and anti-inflammatory, etc.
WO2014006625A1 Pharmaceutical composition comprising amino-phenyl- acetic acid octadec-(z)-9-enyl ester and use thereof for treating tumors The present invention relates to the compound amino-phenyl-acetic acid octadec- (Z)-9-enyl ester, an enantiomer thereof or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising it, for use in the treatment of tumors and metastases, and to methods for treating a tumor or metastases comprising administering said compound to a subject in need thereof. The present invention particularly relates to said compound when it is dissolved in an ethanol solution.
US7323468 as modulators of receptor tyrosine kinases and cytoplasmic tyrosine and serine/threonine kinases; can bind both to active and also to non-active kinases and therefore influence the signal transduction The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general Formula I, their preparation and use as medicaments, in particular for the treatment of malignant and other disorders based on pathological cell proliferations.
US20050152959 Use of a lysolipid for the preparation of a composition for transfection of a polynucleotide into a cell The present invention relates to the use of at least one lysolipid for the preparation of a composition for improving transfection or transduction of a polynucleotide into a cell. Such a composition is useful in gene therapy, vaccination, and any therapeutic or prophylactic situation in which a gene-based product is administered to cells in vivo.
WO2010110328A1 Readily water-soluble isoquercitrin composition Disclosed is a method for improving the solubility of isoquercitrin in water. Also disclosed is a readily water-soluble isoquercitrin composition which is improved in the solubility in water by the method. Specifically disclosed is a method for preparing an isoquercitrin inclusion product, which comprises including isoquercitrin in γ-cyclodextrin in the proportion of 2 to 10 mol of γ-cyclodextrin to 1 mol of isoquercitrin.
US20090017129 Dead Sea minerals enriched anti-inflammatory pharmaceutical composition for treatment of cutaneous dryness, itching, peeling and tightness, especially in hemodialysis patients and preparation and treatment methods thereof This invention relates to Dead Sea anti-inflammatory medicaments or cosmetics for treatment of anti-inflammatory conditions; for example, cutaneous dryness, itching, peeling, and tightness, especially in hemodialysis patients. Methods for the preparation of and methods of treatment using these medicaments or cosmetics are also provided.
US20090280164 Therapy for human cancers using cisplatin and other drugs or genes encapsulated into liposomes A method for encapsulating cisplatin and other positively-charged drugs into liposomes having a different lipid composition between their inner and outer membrane bilayers is disclosed. The liposomes are able to reach primary tumors and their metastases after intravenous injection to animals and humans. The encapsulated cisplatin has a high therapeutic efficacy in eradicating a variety of solid human tumors including but not limited to breast carcinoma and prostate carcinoma. Combination of the encapsulated cisplatin with encapsulated doxorubicin or with other antineoplastic drugs are claimed to be of therapeutic value. Also of therapeutic value in cancer eradication are claimed to be combinations of encapsulated cisplatin with a number of anticancer genes including but not limited to p53, IL-2, IL-12, angiostatin, and oncostatin encapsulated into liposomes as well as combinations of encapsulated cisplatin with HSV-tk plus encapsulated ganciclovir.
WO2012157721A1 Liposome containing pyrroloquinoline quinone and sugar The purpose of the present invention is to provide: a composition which enables the expansion of the concentration range in which pyrroloquinoline quinone can exhibit a cell proliferation promoting function; and a process for producing the composition with high efficiency. The present invention provides: a liposome composition which contains pyrroloquinoline quinone or a salt thereof and a sugar and also contains liposomes having particle diameters ranging from 1 to 10 μm in an amount of 50% or more; and a process for producing the liposome composition.
WO2008046758A3 Imidazolone and imidazolidinone derivatives as 11b-hsd1 inhibitors for diabetes Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
CN101305988A Compound alendronate sodium vitamine D3 orally disintegrating tablets and preparation method thereof The invention relates to compound alendronate sodium vitamin D3 orally-disintegrating tablets used for preventing and treating stmenopausal osteoporosis and a preparation method thereof, aims to provide a novel preparation, i.e. the compound alendronate sodium vitamin D3 orally-disintegrating tablets to patients and medical workers; wherein, the compound alendronate sodium vitamin D3 orally-disintegrating tablets have fast absorption and high bioavailability, need no water when in administration, have little intestinal residue and insignificant side effects, and avoid the first-pass effect in liver sausage. Alendronate sodium vitamin D3 is used as a raw material, auxiliary materials are added in, and the alendronate sodium vitamin D3 orally-disintegrating tablets are prepared according to the technical means.
CN101103975A Phenytoin sodium powder injection and preparation method thereof The invention discloses phenytoin sodium powder injection and the preparation method, relating to power injection for treating falling sickness and relating to the preparation method of the power injection. The invention is characterized in that the phenytoin sodium powder injection contains an active ingredient phenytoin and latent solvent arginine; the arginine is L-arginine or R-arginine. The phenytoin sodium powder injection in the invention, with the arginine as the latent solvent has the advantages that the dissolution is very quick; the clarity is obviously increased; no side effects are produced to patients so that the security of the injection use is increased; the lower pH than the original phenytoin sodium carbonate powder injection helps reduce thrill to the injection site and reduce pain for patients; the concentration of sodions are reduced, therefore the injection can be used to the patient who is limited to absorb sodions.
WO2013123569A1 Formulation of doxylamine and pyridoxine and/or metabolites or salts thereof A dual release oral dosage system/dosage form comprising an immediate release component/composition and a delayed release component/composition is described. Each of the immediate release component/composition and delayed release component/composition comprises one or more of doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof, and one or more of pyridoxine, a salt thereof, a metabolite thereof and/or a salt of the metabolite. The dual release oral dosage system/dosage form exhibits an improved pharmacokinetic profile relative to the current Diclectin® formulation and is useful for example for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting in pregnancy (NVP).
WO2012044162A1 Fat composition for programming immune response The present invention relates to a method for enhancing vaccination response and/or preventing infections in a human subject later in life, by administering said human subject a nutritional composition with a specific fat composition having a defined weight ratio of linoleic acid to alpha - linolenic acid when said human subject is an infant with an age between 0 and 36 months.
CN101919859A Medicinal composition containing pentoxifyllinum and etodolic acid and application thereof The invention belongs to the field of medicaments and particularly relates to a medicinal composition containing pentoxifyllinum and etodolic acid and application thereof. The medicinal composition disclosed by the invention contains two active ingredients, namely, the pentoxifyllinum and the etodolic acid in a ratio of 0.01-10:1, preferably 0.05-2:1. A large number of experiment researches prove that the medicinal composition of the invention has a remarkable effect of treating arthritis and plays a better role in improving a rat hemorrhoids model.
EP1585507A2 The use of estrogen receptor alpha modulators for the treatment of multiphe sclerosis The present invention provides methods of treating an autoimmune pathology in a mammal, comprising administering an agent with estrogen receptor a agonist activity in particular a selective estrogen receptor modulator, to the mammal in an amount sufficient to decrease production of TH-1 and/or TH-2 cytokines. Also provided is a method of selecting compounds useful for the treatment of multiple sclerosis, comprising selecting a compound which has estrogen receptor a agonist activity.
CA2232230C Phosphopantetheinyl transferases and uses thereof The invention pertains to isolated phosphopantetheinyl transferases, such as the E. coli acyl carrier protein synthase, which transfer a phosphopantetheinyl group onto a substrate. The enzyme can be purified from a natural source, produced recombinantly, or synthetically. Accordingly, the invention provides compositions and kits including phosphopantetheinyl transferases and host cells expressing phosphopantetheinyl transferases. The invention also provides nucleic acids encoding phosphopantetheinyl transferases and vectors comprising such nucleic acids. The invention further provides methods for phosphopantetheinylating a substrate in vitro or in vivo and methods for producing antibiotics in vitro or in vivo.
US20130028912 Tweak/fn14 system regulates skeletal muscle atrophy and regeneration The invention provides methods for preventing loss and augmenting regeneration of skeletal muscle by decreasing the activity of the TWEAK/Fn14 system.
US20080132440 Vitamin D or vitamin C complex with polyglutamic acid; improved stability; food, beverage, cosmetic; esterification The present invention relates to PGA-vitamin complex containing poly-γ-glutamic acid(PGA), vitamin preparations containing said PGA-vitamin complex or cosmetic compositions. The inventive PGA-vitamin complex having excellent hygroscopicity, moisturizing property and skin compatibility, which is a complex of poly-γ-glutamic acid and vitamin, has the effect of sustained-release as well as improves stability of vitamin having the functions, such as promotion of metabolism, anti-oxidation effect, protection of cell wall, increasing immunity, prevention of dry skin and keratinization, anti-wrinkles and moisturizing skin, thereby being useful as cosmetic compositions and sustained-release vitamin preparations for various applications.
US20100234412 Buprenorphine Derivatives and Uses Thereof Ester derivatives of the phenolic hydroxyl group of buprenorphine can be used in the treatment of opiate dependency and/or moderate to severe pain. The esters have an enhanced bioavailability, an enhanced duration of action, and a reduced abuse potential.
US20080069830 Isolation Dna; nucleotide sequences; genetic engineering The invention comprises novel DNA, protein, and peptide sequences and novel vaccines, therapeutics and antibodies created with the novel DNA and peptides to prevent or treat SARS by administration of recombinant proteins, synthetic peptides, recombinant viruses, recombinant bacteria, DNA plasmids, RNA plasmids, or other molecular constructs or delivery systems.
WO2011001115A1 Novel 6-morpholin-4-yl-pyrimidin-4-(3h)-one derivatives, and the pharmaceutical preparation thereof as akt(pkb) phosphorylation inhibitors The invention relates to the novel materials of formula (I), where: Z is an optionally substituted O-, -NH, Ncycloalkyl, or Nalkou N-phenyl; n is 0 to 4; R1 is H, Hal, hydroxyl, alkyl, or alkoxy; the alkyl or alkoxy radicals being optionally substituted; R1 can be a phenyl group fused with the phenyl having R1 to form naphthyl; R2 and R3 are H, Hal, or alkyl optionally substituted by one or more halogen atoms; and R4 is H. Said materials can be in any isomeric form and the salts thereof, and are intended for drugs, in particular as AKT(PKB) phosphorylation inhibitors.
EP2230235A1 Botryosphaerones, novel depsidones and their use as medicaments The present invention describes novel compounds (depsidones) of formulas (I) and (1a) as well as their use for the treatment of bacterial infections, fungal diseases (mycosis) or cancer.
WO2014013181A1 Thiophene derivatives used in the treatment of diabetes The invention relates to a thiophene derivative of the following general formula (I) or an enantiomer, diastereoisomer, hydrate, solvate, tautomer, racemic mixture or pharmaceutically acceptable salt thereof, and the use of same as a medicament especially for the treatment and/or prevention of diabetes, the complications thereof and/or associated pathologies, advantageously type 2 diabetes and hyperglycemia.
US20070117788 Combination of a dopamine D2-receptor agonist and tiotropium or a derivative therof for treating obstructive airways and other inflammatory diseases The present invention relates to a combination of therapeutic agents useful in the treatment of obstructive airways and other inflammatory diseases comprising (I) a dopamine D2-receptor agonist that is therapeutically effective in the treatment of said diseases when administered by inhalation; together with (II) an anti-cholinergic agent consisting of a member selected from the group consisting of tiotropium and derivatives thereof that is therapeutically effective in the treatment of said diseases when administered by inhalation; as well as to a method of treating said obstructive airways and other inflammatory diseases comprising administering to said mammal by inhalation a therapeutically effective amount of said combination of therapeutic agents; and a pharmaceutical composition comprising a pharmaceutically acceptable carrier together with said combination of therapeutic agents; and a package containing a pharmaceutical composition for insertion into a device capable of simultaneous or sequential delivery of said pharmaceutical composition in the form of an aerosol or dry powder dispersion to said mammal, where said device is a metered dose inhaler or a dry powder inhaler. It is preferred that said dopamine D2-receptor agonist component be bromocriptine mesylate, naxagolide hydrochloride, cabergoline, pergolide mesylate, quinpirole hydrochloride, or ropinirole hydrochloride; and that said anti-cholinergic agent component be tiotropium bromide.
CN101129401A Nano antibiotic montmorillonite and method of preparing the same The invention relates to a nanometer antibiotic montmorillonite and its preparing process, wherein the nanometer antibiotic montmorillonite comprises montmorillonite 100 weight parts and antibacterial drugs 10-45 weight parts. The preparing process comprises steps of mixing Na-montmorillonite and antibacterial drugs, charging solvent and stirring, forming stable suspension, filtering, removing the solvent, finally drying and ball-grinding.
US20120141471 Methods of Inhibiting Metastasis from Cancer The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one CX3CR1 or fractalkine antagonist.
US20100105754 5-(4phenyl)prolinamide for treatment of epilepsy The invention provides a compound of formula (I), a solvate, a salt or prodrug thereof, useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels.
CN1739584A Phosphatide granule with subsidiary function of reducing blood fat The phosphatide granule with subsidiary function of reducing blood fat consists of lecithin 16-60 wt%, tea polyphenol 1.0-2.5 wt%, ginkgo extract with 24 % over total flavone glycoside 0.39-1.5 wt%, vitamin C 1-5 wt%, vitamin E 0.16-1.5 wt%, vitamin B1 0.02-0.2 wt%, vitamin B2 0.02-0.2 wt% and starch 29.1-91.41 wt%. The present invention has several health functions, including emulsifying blood fat, preventing oxidation, accelerating fat metabolism and eliminating fat toxin, and thus can lower blood fat, raise bodyí»s immunity and strengthen physique.
WO2007012183A1 Process for the production of bicalutamide A process which includes the reacting of sodium perborate with N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)thio]-2-hydroxy- 2-methylpropanamide to form bicalutamide. Said process may comprise the reaction of N-[4-cyano-3-(trifluoromethyl)phenyl]-2- methyloxiranecarboxamide with 4-fluorobenzenethiol in the presence of a base, water and a first solvent that is water miscible to form N-[4- cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)thio]-2-hydroxy-2-methylpropanamide, and reacting the N-[4-cyano-3- (trifluoromethyl)phenyl]-3-[(4-fluorophenyl)thio]-2-hydroxy-2-methylpropanamide with sodium perborate in a second solvent. The process is efficient, inexpensive, environmentally friendly and produces bicalutamide in good yield.
US7427627 N-(4-(4-methylthiazol-5-yl) pyrimidin-2-yl)-N-phenylamines as antiproliferative compounds The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.
US6852714 (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6-Alk2-(b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.
CN1859916A Drugs, foods and drinks for ameliorating hyperglycemia Compounds having effects of ameliorating hyperglycemia and lowering hemoglobin Alc level such as 4-methylcholest-7-en-3-ol, 4-methylergost-7-en-3-ol and 4-methylstigmast-7-en-3-ol are employed as the active ingredient of drugs, foods or drinks for ameliorating hyperglycemia.
WO2006040646A1 Benzimidazole or indole amides as inhibitors of pin1 The invention relates to compounds of the formula (1) and to pharmaceutically acceptable salts and solvates thereof, wherein the variables are defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula (1) and to pharmaceutical compositions for treating such disorders that contain the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1).
US20070269421 Diagnostics and Therapeutics for Diseases Associated with Plasma Glutamate Carboxypeptidase (Pgcp) The invention provides a human PGCP which is associated with the cardiovascular diseases, endocrinological diseases, metabolic diseases, cancer, inflammation, gastroenterological diseases, hematological diseases, respiratory diseases, muscle-skeleton diseases, neurological diseases and urologial diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular diseases, endocrinological diseases, metabolic diseases, cancer, inflammation, gastroenterological diseases, hematological diseases, respiratory diseases, muscle-skeleton diseases, neurological diseases and urologial diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of PGCP as well as pharmaceutical compositions comprising such compounds.
US20120208795 Compositions and methods for the treatment of addiction and other neuropsychiatric disorders The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to an activity) as well as to alleviate some of the symptoms experienced during menopause or associated with the menstrual cycle. Regardless of the precise formulation, the compositions of the invention can include at least one active ingredient that targets the hypothalamopituitary-adrenal (HPA) axis and at least one active ingredient that targets the prefrontal cortex. Either or both of these types of agents can be combined with an agent that inhibits activity in the sympathetic nervous system. Thus, the compositions or combination pharmacotherapies can also include an agent that inhibits a beta-adrenergic receptor or that otherwise acts as an anti-hypertensive or anxiolytic agent.
WO2014042238A1 Sulfonamide compound The invention provides a novel sulfonamide compound useful as a drug having a TRPM8-blocking effect. Specifically, the invention provides a sulfonamide compound represented by formula (I) or a pharmaceutically acceptable salt thereof. (In the formula, ring A is formula (i), (ii), or (ix), R4 is an optionally substituted alkyl, X1 and X2 are each independently tetrazolyl, tetrazolinonyl, optionally substituted triazolyl, triazolinonyl, oxadiazolonyl, optionally substituted alkanoylaminomethyl, or optionally substituted alkylsulfonylaminomethyl, or R4 and X2 bond to each other at the ends and form indazolinonyl or benzoisoxazolonyl with the adjacent benzene; other symbols are as stated in the specification.)
CN101069741A Medical radiation-ray preventive spray agent The present invention discloses a medical ray protection spray capable of protecting human body against injury due to radiation ray The effective components of said spray include (by wt%) 0.002-0.3% of superoxide dismutase, 0.01% of pentose, 0.1% of polyethylene glycol 6000, 0.1% of witamin C 0.1% of potassium sorbate and the rest is distilled water. Besides, said invention also provides its preparation method.
CN101406485A Method for producing decoction for quickly relieving bowels The invention discloses a method for producing soup for purging urine and feces quickly in the technical field. With the method, urine and feces diseases can be purged within a few hours. The method is realized through the following technical proposal: putting honey in a porcelain and putting the porcelain in a steamer for steaming at a temperature of between 70 and 90 DEG C for 30 to 90 minutes; grinding Glauber's salt finely, mixing well boiling soup, then putting the honey, the Glauber's salt and the boiling soup together to be stirred for 5 to 10 minutes, keeping stand the mixture for 30 minutes and then heating the mixture for 10 to 20 minutes, and stopping boiling to cool the mixture so as to obtain a finished product of the soup.
CN102430036A Burn and scald antibacterial and pain-relieving ointment The invention relates to a burn and scald antibacterial and pain-relieving ointment, which is an externally applied ointment for treating burns and scalds. The ointment consists of rhubarb, garden burnet root, aloe, Chinese arborvitae twig, angelica dahurica, phellodendron, fineleaf schizonepeta herb, purple flower holly leaf, rehmannia root, cicada slough, diverse wormwood herb, hairyvein agrimonia herb and bud, calamine, gypsum rubrum, borneol, beeswax and sesame oil, has the effects of removing heat, cooling blood, relieving pain, eliminating necrotic tissue, promoting granulation, stopping bleeding, resisting permeability, and the like, has a good effect, quick response, the effective rate of 100 percent, and the effect of treating both symptoms and root causes when used for treating burns and scalds, can fulfill the aim that the burns and scalds are difficult to relapse after being cured, also can be used for treating knife wounds, bruise, bedsore, woman vulvar and vaginal ulcers, wounds after a haemorrhoid operation, various skin-related operation wounds, skin infection and all body surface ulcers, and has a certain curative effect on mosquito bite and dry tinea.
EP2282756A1 Methods of diagnosing, preventing and treating bone mass diseases The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPHl inhibitors or serotonin receptor antagonists.
US20100041759 Multi-phase release potassium guaiacolsulfonate compositions Formulations have been developed administering a guaiacolsulfonate salt, preferably potassium salt, in multi-phases. In a preferred embodiment, the formulation contains potassium guaiacolsulfonate in an immediate release (“IR”) form and a sustained or delayed release (“DR”) form and/or pulsed release (“PR”) form. In another embodiment, the potassium guaiacolsulfonate is released in a gradient, decreasing the side effects associated with rapidly elevated blood levels. In another embodiment, the drug is bound to an ion-exchange resin, which can be suspended in a liquid or incorporated into a matrix for delayed, sustained and/or pulsed release. Dosage unit forms may be tablets, gels, liquids, capsules, beads, microparticles, films or lozenges. Multi-phase delivery can also be achieved through the use of a kit that provides for dosage escalation. The formulations are useful in the treatment of one or more symptoms of coughs, colds, sinusitis and other respiratory illnesses. The formulations are also useful in the treatment or relief of fibromyalgia, pain, and Irritable Bowel Syndrome.
US20120196301 Use of binding partners for 5-ht5 receptors for the treatment of neurodegenerative and neuropsychiatric disorders The present invention relates to the use of binding partners for 5-HT5 receptors for the treatment of neuropathological, in particular neurodegenerative and/or neuropsychiatric, disorders, which can occur, in particular, in cerebral ischemia, stroke, epilepsy and seizures in general, chronic schizophrenia, other psychotic disorders, dementia, in particular Alzheimer's dementia, demyelinizing disorders, in particular multiple sclerosis, and brain tumors. The invention also relates to processes for the identification and characterization of such binding partners, in particular in the form of screening processes.
US20080176891 N-(2-Aminoethyl)-4-(2-ethyl-1H-pyrrolo[2,3-b]pyridin-4-yl)benzene-sulfonamide; respiratory disorders; rheumatoid arthritis The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
US20090124648 Such as trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide and novel salts, hydrates and polymorphs thereof; neuropeptide y5 (NPY5) The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide and novel salts, hydrates and polymorphs thereof.
WO2011070250A1 Novel azabicyclo[3.2.0]hept-3-yl derivatives, method for preparing same, and pharmaceutical compositions containing same The invention relates to compounds of formula (I), where ALK is an alkylene chain, and W is a grouping (I') or (I''), where R and R' are as defined in the description. The invention is of use as a drug.
US20080058386 1-(4-Methoxy-benzenesulfonyl)-2,3-dihydro-1H-indol-7-ylamine; inhibiting tubulin polymerization; anticarcinogenic; mitotic arrest of microtubule structure, neovascularization; angiogenesis inhibitor: atherosclerosis, rheumatoid arthritis or Crohn's disease, diabetic retinopathy, psoriasis A series of indoline-sulfonamide compounds is disclosed. The formula of indoline-sulfonamide compounds is shown as formula (I). In formula (I), R1 is H or halogen; R2 is Ar, Ar—C(O)—, Ar—CH2—, Ar—SO2—, Ar—O—C(O), or R″—C(O)—, and Ar is a substituted or unsubstituted C5-C20 aryl, cyclyl, heterocyclyl, or heteroaryl, R′ and R″ independently is C1-C10 alkyl, or C1-C10 alkoxyl; and R3 is C5-C15 aryl or C1-C10 alkyl. The indoline-sulfonamide compounds disclosed in the present invention are characterized in inhibiting tubulin polymerization, and treating cancers and other tubulin polymerization-related disorders with a suitable pharmaceutical acceptable carrier.
CN101496887A Medicament for treating acute hot, itching and wet severe type and chronic urticaria The invention discloses a drug for treating acute heat and tickle predominating type, dampness predominating type and chronic urticaria, which is prepared from 30 bulk drugs according to certain weight ratio including angelica, radix sileris, shell of areca nut, white batryticated silkworm, radix rehmanniae, bamboo leaf, astraolylis lancea formalyrata, cortex magnoliae officinalis, and the like. The drug can be prepared into any of internally-administrated dosage forms in common use. The drug has functions of invigorating the spleen and treating with both elimination and reinforcement, and has obvious curative effects of treating the acute heat and tickle predominating type urticaria, cute dampness predominating type urticaria and chronic urticaria, wherein most of urticaria patients are healed with difficult relapse.
EP1996210A2 Oral hygiene products and method of using the same The present invention is directed towards a composition for highly efficient and quick plaque and tartar removal and inhibition including pure ascorbic acid crystals and/or granulars (vitamin C) and an enamel repairing composition such as hydroxyapatÊte. The composition can contain from about 10% up to 90% of ascorbic acid without compromising the tooth enamel because hydroxyapatite will repair any damage to the enamel. The composition can be used as dental powder, toothpaste, mouthwash, mouth spray and chewing gum in order to cover a wide range of consumers in different settings.
EP2004139A1 Compositions, methods, and kits using adenosine and inosine in combination for diagnosis and treatment The present disclosure relates to compositions, methods, and kits using adenosine and inosine in combination for diagnosis and treatment.
CN102895538A Preparation technology and production method for integrated new formulation of white tiger and genseng decoction The present invention relates to a preparation technology and a production method for an integrated new formulation of a white tiger and genseng decoction, wherein the raw materials of active ingredients comprise: 18 parts by weight of anemarrhena, 30 parts by weight of gypsum, 6 parts by weight of licorice, 12 parts by weight of polished rice, and 9 parts by weight of genseng. The production process of the integrated new formulation of white tiger and genseng decoction comprises the following steps of: supersonic air-jet crushing, alcohol-water extraction, ultrasonic crushing extraction, water decocting concentration, supersonic spray drying, nanometer grinding, high pressure homogenization, nano particle preparation and the like. According to the invention, the advantages, such as multi-synergism, multi-target, embodied by a nano-carrier coupling technique, are focused to be taken of. After the integrated new formulation of white tiger and genseng decoction is subjected to scale production, the production cost can be greatly reduced, the quality of products is greatly improved and the targeting property, and the sustained and controlled release performance of the medicament are enhanced. The internal and external administration of the integrated new formulation of white tiger and genseng decoction can be realized simultaneously, and the medicament can be separately taken in four time slices according to the midnight-noon ebb-flow and qi and the blood flowing rule of a human body. The integrated new formulation of white tiger and genseng decoction can be further prepared into films and transdermal agents, which are respectively stuck to different parts of a human body according to the midnight-noon ebb-flow and qi and blood flowing rule of the human body, and can be directly absorbed through skin.
EP1747782A1 Products for topical application comprising lysophospholipids and fatty acids It is described a product containing at least one lysophospholipid and at least one fatty acid, as a combined preparation for simultaneous, separate or sequential use, to be topically applied, in order to temporarily and reversibly inhibit a neuromuscular junction or the release of acetylcholine from autonomic nerve endings; this product can be used for treating hyperhidrosis conditions and for the cosmetic treatment of facial and other body wrinkles and, in general, human syndromes caused by the hyperactivity of peripheral nerve terminals.
CN103655746A Externally-used medicinal ointment for treating alopecia and preparation method thereof The invention provides externally-used medicinal ointment for treating alopecia. The externally-used medicinal ointment is prepared from the following raw materials in percentage by weight: 0.1-0.5% of angelica sinensis root extract, 0.1-0.5% of polygonum multiflorum extract, 0.05-0.2% of ginseng root extract, 25-35% of cod liver oil, 25-35% of nano-zinc oxide, 0.3-0.8% of calamine, 0.5-2% of borneol, 15-20% of ethylhexyl palmitate, 10-15% of glyceryl stearate and 5-10% of cetostearyl alcohol. The invention further provides a preparation method of the externally-used medicinal ointment for treating the alopecia. The externally-used medicinal ointment is simple in preparation process, convenient to use without massaging, free of toxic and side effects and quick in effect, and has a significant effect on alopecia totalis, alopecia areata, alopecia universalis, in particular seborrheic alopecia; after hair begins to grow, functions of hair follicles are stable, and after stopping using the ointment, the functions of the hair follicles can be kept for a long time; and the ointment has no special requirement on age and gender and has a relatively satisfactory effect on women and the elderly.
US20050106152 Using protein antagonist; amino acid sequence; antisense nucleotide; inducing apoptosis A compound or its salt that regulates the activities of a protein having the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, an antisense nucleotide containing a base sequence or a part thereof which is complementary or substantially complementary io the base sequence of a DNA encoding a protein or its partial peptide having the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, etc. can be used as preventive/therapeutic agents for cancer, etc.
US7019007 CCR-3 receptor antagonists (I) The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.
US20110144122 Derivatives of 2-oxoalkyl-1-piperazin-2-one, preparation method thereof and therapeutic use of same The present invention relates to derivatives of 4-{2-[phenyl-3,6-dihydropyridin-1-yl]-2-oxoalkyl}-1-piperazin-2-one and 4-{2-[phenyl-2,5-dihydropyrrol-1-yl]-2-oxoalkyl}-1-piperazin-2-one having general formula (I): in which A, B, m, R3 and n are as defined herein. The invention also relates to the preparation thereof and to the therapeutic use thereof.
CA2173505C Use of penciclovir for the treatment of post-herpetic neuralgia A method for the treatment of PHN in mammals, including humans, which method comprises administering an effective amount of a compound of formula (A), or a bioprecursor, or a pharmaceutically acceptable salt, phosphate ester and/or acyl derivative of either of the foregoing.
CN1820755A Medicinal composition of cefuroxime and ambroxol hydrochloride The present invention relates to medicine composition of cefuroxime and ambroxol hydrochloride. The medicine composition contains cefuroxime and ambroxol hydrochloride in the weight ratio of 125-1500 to 15í½60, preferably 250 to 15, or 750 to 30. The medicine composition of cefuroxime and ambroxol hydrochloride may be prepared into injection or orally taken preparation through different preparation processes, the injection adopts the sodium salt of cefuroxime, and the orally taken preparation takes ethyl acetate of cefuroxime. The medicine composition of cefuroxime and ambroxol hydrochloride is superior to available compound ambroxol hydrochloride preparation, with drug resistance, instability in beta-lactamase and other demerits, and has determined curative effect on respiratory tract infection.
WO2010058318A1 1-oxa-8-azaspiro [4, 5 ] decane- 8 -carboxamide compounds as faah inhibitors Provided herein are 1-oxa-8-azaspiro[4.5]decane-8-carboxamide compounds of formula I wherein Ar1, Ar2, R1, R2, R3 and R4 are as defined herein and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.
CN101611058A PRLR-specific antibody and uses thereof PRLR-specific antibodies are provided, along with pharmaceutical compositions containing such antibody, kits containing a pharmaceutical composition, and methods of preventing and treating cancer.
US7846927 N,N′-diphenylurea derivatives suitable as kinase inhibitors Compounds of the formula (I), in which R1, R3 and X have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.
US20110237658 Compound and method for the treatment of pain The disclosure herein provides a compound of formula 1. The disclosure also provides a method of synthesizing the compound of formula 1. The compound of formula 1 or its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof may be formulated as pharmaceutical composition. The pharmaceutical composition of compound of formula 1 or the final compound may be formulated for non-invasive peroral, topical (example transdermal), enteral, transmucosal, targeted delivery, sustained release delivery, delayed release, pulsed release and parenteral methods. Such compositions may be used to treat chronic pain manifested with chronic diseases or its associated complications.
US20090304651 Insulin-Like Growth Factor II (IGF-II) Binding Factors This invention relates to modified IGF-II binding domains of the Insulin-like Growth Factor 2 Receptor (IGF2R) which have enhanced binding affinity for IGF-II relative to the wild type IGF-II binding domain. Suitable IGF-II binding domains may be modified, for example, by substituting residue E1544 for a non-acidic residue. These modified domains may be useful in the sequestration of Insulin-like Growth Factor II (IGF-II), for example, in the treatment of cancer.
WO2006105725A1 A combination of luteolin and one of pt chemotherapeutics A pharmaceutical composition contains luteolin and one of Pt chemotherapeutics comprising cisplatin, carboplatin and oxaliplatin. The combination of luteolin and Pt chemotherapeutics has the synergistic effect in treating tumor, it may be used for the manufacture of medicine in treating tumor thereby.
US20090075929 Ig20 splice variants therapeutics for cancer Methods and compositions inhibit the growth of cancer cells by selectively down-regulating the expression of an IG20 splice variant including MADD. Specific knock-down of MADD splice variant resulted in the apoptosis of cancer cells. Interfering RNAs including small hairpin RNAs (shRNA) to down-regulate MADD expression in vivo are disclosed. Inhibition of MADD phosphorylation by Akt results in activation of cancer cell death. Down-regulation of MADD expression results in switching to apoptotic mode due to lack of MAPK activation upon TNF-α-based induction.
US20070269525 O/W Gel Compositions Comprising Wax An oil in water gel composition including (a) from about 0.05% to about 5% by weight of at least one polymeric gel former selected from the group consisting of acrylic acid, acrylamide, homopolymers and copolymers of acrylic acid, homopolymers and copolymers of acrylamide, derivatives thereof, and mixtures thereof; (b) from about 0.1% to about 10% by weight of at least one wax component with a melting point of at least 30° C.; (c) from about 1% to about 30% by weight of an oil component which is liquid at 25° C.; and (d) from about 60% to about 95% by weight of water, with the proviso that the composition is free from anionic and cationic emulsifiers and surfactants is provided. Processes for producing the compositions and incorporation of the compositions into a cosmetic formulation are also provided.
CN101670008A Deer fetus film and manufacturing method thereof The invention discloses a deer fetus film and a manufacturing method thereof. The deer fetus film is characterized in that the formula of the deer fetus film comprises the following components in portion by weight: 40 portions of dried deer fetus powder, 5 portions of dried antler slice powder, 100 portions of donkey-hide glue, 20 portions of deer bone powder, 150 portions of black sesame, 60 portions of jujube, 20 portions of finger citron, 125 portions of raw crystal sugar, 500 portions of yellow rice wine, and 1,000 portions of water. The manufacturing method comprises the following steps:processing deer fetus, antler, donkey-hide glue, deer bone powder, black sesame, jujube, finger citron and the like; successively adding the dried deer fetus powder, dried antler slice powder, donkey-hide glue, deer bone powder, yellow rice wine, finger citron, jujube, black sesame and raw crystal sugar into the water of 80 to 90 DEG C in sequence according to the proportion of the formula; and stirring the mixture evenly, decocting the mixture till sterilizing, spreading the mixture for cooling, thoroughly cooling the mixture, and slicing the mixture to obtain the deer fetus film. The deer fetus film created by the manufacturing method has the effects of tonifying sufficiency, resisting fatigue, boosting essence blood, releasing sinus toxin and drug toxin and supplementing kidney qi, hasbetter warming function for people who always get cold on hands and feet, and can build the body after long-term administration.
WO2014014841A1 Pharmaceutical compositions of (r)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration thereof A pharmaceutical composition comprising Compound 1, (R)- 1 -(2,2- difluorobenzo[d] [ 1,3]dioxol-5-yl)-N-( 1 -(2,3-dihydroxypropyl)-6-fluoro-2-( 1 -hydroxy-2- methylpropan-2-yl)- l H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from : a filler, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.
US20080260861 Modulating Lymphatic Function Methods and compositions for modulating lymphatic function, e.g., by altering NO levels, are disclosed.
US20100316575 Modulating body weight This document provides methods and materials related to modulating body weight. For example, methods and materials related to treating obesity, reducing body weight, preventing body weight gain, increasing body weight, and identifying agents having the ability to treat obesity and reduce body weight are provided.
US20120237615 Pharmaceutical compositions of o-nitro compounds The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.
CN103735507A Method for preparation of paclitaxel liposome by ethanol injection The invention discloses a method for preparation of a paclitaxel liposome by ethanol injection. The specific steps include: firstly, accurately weighing objective raw materials, then adding cholesterol and soybean phospholipid for injection; conducting ultrasonic wave for 3min till complete dissolution; performing heat bath to the mixture for at least 10min; carrying out magnetic stirring under a constant temperature for at least half an hour; injecting chlorine gas; carrying out filtration concentration and constant volume setting, then performing filtering on filter paper, and discarding the supernatant; adding glucose powder, performing stirring again, and conducting high speed centrifugation; taking the precipitate, and conducting drying, thus obtaining the paclitaxel liposome. The method provided by the invention has the advantages of: simple operation, easily controllable size and high yield, and is scientific and feasible.
CN102204913B Application of ligustrazine derivative in preparation of medicament for treating melanoma The invention belongs to the field of pharmacy and discloses the application of a ligustrazine derivative (2,5-dimethylol-3,6-dimethylpyrazine) to the preparation of an anti-malignant melanoma medicament. The chemical name of the ligustrazine derivative is 2,5-dimethylol-3,6-dimethylpyrazine, wherein the molecular formula is C8H12N2O2. Researches show that the ligustrazine derivative can inhibit the multiplication of melanoma cells (B16F10) and induce cell apoptosis and the like, and can be applied to the anti-malignant melanoma medicament.
CN101095659A Liposome combined medicine and method for preparing the same The invention relates to a liposome compound and the preparing method, which is characterized in that said liposome compound comprises one or several compounds of clindamycinum, fleraxacin, levofloxacin hydrochloride and ciprofloxacin. The toxicity of product is low, medical effect is high and effective prevention of drug resistance generation by pathogenic microorganism.
CA2841404A1 Treatment of angiogenesis disorders This invention concerns pathological angiogenesis and cancer, related treatment methods, and related compositions. Also disclosed are related diagnosis kits and methods.
EP1763511B1 Phenoxyacetic acid derivatives as ppar agonists Novel compounds of the general formula (I), the use of these compounds as phar- maceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPARδ suptype.
US20100291160 Pharmaceutical system for trans-membrane delivery Non-invasive drug delivery systems useful for the absorption of therapeutically active agents through the epithelial membrane are described. The non-invasive drug delivery system delivers a therapeutic active agent with an ionizable, or ionized, metal, transition metal or metal-containing vehicle. The non-invasive drug delivery system may also have a pH adjustable vehicle which facilitates the absorption of the therapeutic agents by altering the pH of the non-invasive drug delivery system at the site of administration. Also disclosed is a method for the pH “sweeping” of the administered therapeutic active agent to provide a consistent and reproducible absorption of the active agent. Certain formulations utilize low doses of active agents without altering the active agents from their current or previous form.
WO2012020421A1 A novel process for preparation of bosentan A novel ammonium salt of Bosentan of formula (VIII); has been disclosed. The salt may be either crystalline or amorphous or mixture of Crystalline and amorphous form. A novel single pot process for the preparations of ammonium salt of Bosentan has been disclosed. The process comprises reacting the 4,6-dichloro-5-(2-methoxyphenoxy)-2,2'- bipyrimidine with 4-tert-butylbenzenesulfonamide in the presence of solvent and a base; adding ethylene glycol to the reaction mass and isolating the ammonium salt of Bosentan. The ammonium salt of Bosentan is converted into Bosentan and further into Bosentan Monohydrate which are substantially free from dimer impurity and 6-hydroxy impurity.
EP1646638A2 11-12 bicyclic erythromycin derivatives The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
CN102178668A Application of linoleic acid in preparing human papillomavirus (HPV) resisting medicament The invention provides application of linoleic acid in preparing a human papillomavirus resisting (HPV) medicament. In the application, the linoleic acid can be a soluble solution prepared by using linoleic acid, or an extract extracted from natural plants. The linoleic acid has trend of inhibiting Hacat cell multiplication, and the inhibiting trend of the linoleic acid increases along with extension of the acting time of the medicament. Polymerase chain reaction experiments and cytological experiments prove that the linoleic acid has HPV resistance, and plays a role in treating condyloma acuminata (CA).
CN103275035A Benzothiazine compound, and preparation method and anti-tumor purpose thereof The invention relates to the field of pharmaceutical chemistry, in particular to a benzothiazine derivative (I), and a preparation method and an anti-tumor purpose thereof. The definition of Ar is the same as shown in the specification. A pharmacodynamic test proves that the compound with a general formula (I) as shown in the specification has a significant anti-tumor function, and can be used for treating tumors, preferably a small cell lung cancer, a non-small cell lung cancer, a liver cancer, a colon cancer, a rectal cancer, a stomach cancer, a mammary cancer, a skin cancer or a prostatic cancer.
CN103012520A Anti-HBV (Hepatitis B Virus) active compound philippine indican derivative The invention relates to a philippine indican derivative, or a pharmaceutically acceptable salt, ester or solvate thereof. The philippine indican derivative has the structural formula shown in the specification, wherein the glycosyl groups represent glycosyl groups. The philippine indican derivative or the pharmaceutically acceptable salt, ester or solvate thereof can be applied to preparing an anti-HBV medicine.
WO2011033361A3 Combination and composition that contains an antimicrobial, a glucocorticoid and an antimycotic The present invention relates to a topical pharmaceutical composition that comprises the combination of an antimicrobial, a glucocorticoid, an antimycotic and pharmaceutically acceptable vehicles or excipients; the method for producing the composition and the use of said composition for treating localized dermatosis ailments.
EP2190850A1 Small molecule correctors of deltaf508 cftr trafficking This invention provides compounds of Formula I. The compounds are correctors of ΔF508 CFTR trafficking. Also provided are uses of compounds of Formula I for treatment, as well as methods of treatment, of cystic fibrosis.
CN103755724A Penicillin derivatives and applications thereof The invention discloses a (2S,5R,6R)-6-(2,5-dioxo-3-substitued phenyl-1-piperazino)-3,3-dimethyl-7-oxo-4-thio-1-azabicyclo-[3.2.0]heptanes-2-formic acid derivatives or formates thereof, the structural formula is shown in description, wherein R1-R3 are respectively selected from hydrogen, halogen, methyl, methoxyl, hydroxyl, nitryl and azyl. Proved by experiments, the (2S,5R,6R)-6-(2,5-dioxo-3-substitued phenyl-1-piperazino)-3,3-dimethyl-7-oxo-4-thio-1-azabicyclo-[3.2.0]heptanes-2-formic acid derivatives or formates thereof have better in-vivo antibacterial activity, and can be used as active ingredients for preparing antibiotics drugs, thus having better development prospects in the antibiotics drugs.
CN101182563B Method for preparing lactulose by co-immobilized lactose enzyme and glucose isomerase A method for preparing lactulose with co-immobilized lactase and glucose isomerase belongs to the food biotechnology field. The invention utilizes the co-immobilized lactase and the glucose isomerase as the catalysts and takes lactose as the single substrate to convert the lactose and prepare the lactulose under moderate conditions; the unique point of the invention is that the lactase is taken as the substrate and with the cooperative action of the lactase and the glucose isomerase in the reaction, the reaction efficiency for preparing the lactulose is promoted and the byproduct is reduced; moreover, the downstream separation steps are simplified. The invention is characterized by novel thinking, being environment friendly and strong practicability; therefore, the method is a good substitution for the chemical method and free enzyme method for preparing the lactulose.
CN103432090A Cyclovirobuxine D sublingual tablet as well as preparation method and application thereof The invention provides a cyclovirobuxine D sublingual tablet which is a preparation prepared from the following raw materials and auxiliary materials in parts by weight: 0.1-0.2 part of cyclovirobuxine D, 4-7 parts of lactose or pregelatinized starch, 3-5 parts of microcrystalline cellulose and 0.3-0.7 part of low-substituted hydroxypropyl cellulose. The invention further provides a preparation method and an application of the sublingual tablet. The sublingual tablet provided by the invention has small categories of auxiliary materials, high drug concentration, high disintegrating speed and excellent permeable membrane absorption, and can be effectively used for sublingual administration; in addition, after the raw materials and the auxiliary materials are mixed, a special dispersion technology is not needed for processing so that a forming process is simple and convenient, the production cost is low, and the industrial production is beneficial.
CN102416054A Composition for treating onychomycosis and tinea manus and pedis The invention discloses a composition for treating onychomycosis and tinea manus and pedis, which is prepared from the following materials and raw material medicines in part by weight: 30 to 80 parts of 1,000ppm nanosilver solution, 50 to 200 parts of pine oil, 50 to 125 parts of benzoic acid, 50 to 120 parts of rhubarb, 30 to 80 parts of hawthorn and 80 to 160 parts of cuttle bone. The medicinalcomposition disclosed by the invention can treat onychomycosis and tinea manus and pedis and skin infections caused by various enterobacteria, pyogenic bacteria and pathogenic fungi, and has good sterilization effect and quick effectiveness.
EP0651637B1 Control of wound scar production with calmodulin inhibitors or protein kinase c inhibitors This invention pertains to a method for controlling wound scar production by administering a calcium antagonist, alone or in a combination with or followed by a steroid, to the wound site. The method can be used to minimize wound scars, such as hypertrophic wound healing disorders, keloids and burn scar contractures in humans or other mammals, particularly those individually prone to excessive scarring. Calcium antagonist treatment can also be used to control diseases associated with excessive scarring, such as cirrhosis of the liver, constructive pericarditis, Dupuytren's disease of the hand, plantar fibrosis of the foot, and various other fibromatoses.
WO2009031999A1 Fr901464 and analogs with antitumor activity and method for their preparation The present invention provides analogs of FR901464, as well as a methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing.
WO2013124826A1 Oxazolidin- 2 -one compounds and uses thereof as pi3ks inhibitors The present invention relates to oxazolidin-2-one subsituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
CA2242750C Antibodies with reduced net positive charge Antibodies have been modified by chemical conjugation with agents reactive with free amino groups. Among the chemical agents used in connection with the invention are heterobifunctional reagents and biotin. The modified antibodies are also used in the diagnosis and therapy of cancer and other mammalian disease. Diagnostic uses include immunoscintigraphy. The modified antibodies may be further conjugated with labels or biologically active molecules for use in diagnosis and therapy. The modified antibodies may also be formulated into pharmaceutical compositions for these purposes.
US20060204459 Use of tyrosine inhibitors for whitening human skin and treating melanocyted dysfunction associated diseases The present invention relates to a method for whitening human skin and treating melanocyte dysfunction associated diseases comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non-toxic, selective and potent c-kit inhibitor. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.
US20090054482 Method of making and administering quinoline derivatives as anti-cancer agents The present invention relates methods of preparing quinoline derivative compounds, and administering such compounds in the treatment of solid and non-solid tumors, notably on liver cancer.
US20080312250 Combination Comprising a Bcrp Inhibitor and 4- (4-Methylpiperazin-1-Ylmethyl)-N-[4-Methyl-3- (4-Pyridin-3-Yl) Pyrimidin-2-Ylamino) Phenyl] -Benzamide The present invention relates to a combination which comprises a BCRP inhibitor and Compound I of formula (I), in which the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, especially in the delay of progression or treatment of cancer, and to pharmaceutical compositions comprising such combinations.
EP1492787A2 (condensed) pyrimidone and (condensed) pyridone compounds, processes for their preparation, and pharmaceutical compositions containing them Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis. In Formula (I) R1, R2, R3, R4, R5, R6, X and Y are as defined herein.
WO2012100835A1 Methods and compositions for the treatment of aids The application relates to a method for the treatment of a disease caused by HIV infection by administering to a patient in need thereof of a specific inhibitor of the dehydroceramide desaturase. The invention relates as well to compositions comprising a Des-1inhibitor and one or more drugs suitable for the treatment of diseases caused by HIV infection as well as to methods for the identification of compounds suitable for the treatment of said diseases.
CN102018782B Compound cutch sarcogenic oil and preparation method thereof In the formula, cutch is bitter and cool, can stop bleeding, promote tissue regeneration, heal sores and relieve pain and has the main effect of treating all sores; golden thread and wild chrysanthemum remove heat to relieve fire and eliminate toxins; rhubarb promotes blood circulation, eliminates stasis and removes heat to relieve fire; borneol removes heat, eliminates toxins and promotes tissueregeneration; and the medicaments added with cool and moist colza oil can fully protect wounds, reduce swelling, ease pain, perform convergence and promote tissue regeneration, is used for various wounds and rapidly heal the wounds. The compound cutch sarcogenic oil is externally applied on an affected part twice a day.
US7498335 Method of producing an antiangiogenic or vascular permeability reducing effect The invention concerns the use of a quinazoline derivative of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human.
US20120302627 Method of using adenoviral vectors to induce an immune response The invention provides a method of inducing an immune response against a human immunodeficiency virus (HIV) in a mammal. The method comprises administering to the mammal an adenoviral vector composition comprising one or more adenoviral vectors encoding two or more different HIV antigens, the production of which induces an immune response against HIV in the mammal. The invention also provides an adenoviral vector composition comprising four adenoviral vectors encoding an HIV clade A Env protein, an HIV clade B Env protein, an HIV clade C Env protein, and a fusion protein comprising an HIV clade B Gag protein and Pol protein, respectively.
US20080255140 2-(N'-2-amino-3,4-dioxocyclobutenyl)-N-piperazinyl)-pyrimidine-5-hydroxamic acid derivatives; antiproliferative, anticarcinogenic, and antitumor agents; psoriasis; skin, respiratory system, psychological, and genetic disorders; transplant rejection; Alzheimer's and Parkinson's disease; vision defects This invention comprises the novel compounds of formula (I) wherein R1, R2 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
WO2005037187A3 High affinity ligands for influenza virus and methods for their production The present invention relates to long branched poly-N-acetyllactosamines and analogous spacer modified divalent sialosides binding to the large binding site of influenza hemagglutinin. The invention further relates to the method for evaluating the potential of a chemical entity to bind to a molecule or molecular complex comprising a large binding site of influenza hemagglutinin. The invention also provides ligands to influenza hemagglutinin for use in the prevention and/or treatment of influenza.
US20120004245 Compounds for the treatment of posterior segment disorders and diseases The use of certain urea compounds, for the treatment of retinal disorders associated with pathologic ocular angiogenesis and/or neovascularization is disclosed.
WO2014028587A1 Compositions comprising chitosan-drug conjugates and methods of making and using the same The present disclosure relates to nanosized chitosan-statin conjugates, nanosized chitosan-chemotherapeutic agent conjugates, compositions comprising such nanosized chitosan-drug conjugates, and methods of making and using the same. The compositions result in unexpected and dramatic improved bioavailability of the component statin or chemotherapeutic agent.
CN102106862A New application of aspirin The invention discloses a new application of aspirin in treating tinea pedis. The new application method of the aspirin comprises the following concrete steps: firstly grinding the aspirin into powder; and smearing a proper amount of the powder on the fester parts of toes or toe seams, wherein the fester parts is cleaned before smearing is carried out. By virtue of the new application of aspirin in treating the tinea pedis provided by the invention, the recognition of people to the aspirin is broadened. As the aspirin has low price, several cents for one pill of the aspirin sold on the market at present, and one pill can be used for several times, various existing medicaments for treating the tinea pedis can be completely replaced by the aspirin, thus greatly reducing the treatment cost.
EP1133497B1 Crystal modification b of 8-cyano-1- cyclopropyl -7-(1s,6s-2, 8-diazabicyclo 4.3.0]nonan -8-yl)-6- fluoro-1,4- dihydro-4- oxo-3-quinoline carboxylic acid The invention relates to a defined crystal modification of 8-cyano-1- cyclopropyl -7-(1S,6S-2, 8-diazabicyclo [4.3.0]nonan -8-yl)-6- fluoro-1, 4-dihydro-4- oxo-3-quinoline carboxylic acid of formula (I), to methods for producing the same, and to its use in pharmaceutical preparations. The crystal modification can be distinguished from other crystal modifications of 8-cyano-1- cyclopropyl-7- (1S,6S-2,8- diazabicyclo [4.3.0]nonan -8-yl)-6- fluoro-1, 4-dihydro-4- oxo-3-quinoline carboxylic acid of formula (I) by its characteristic X-ray powder diffractogram and its differential thermal diagram (see description).
CN101884614B Preparation of brain targeting chuanxiongzine oral oil package oil nano-emulsion The invention relates to a brain targeting oral oil package oil chuanxiongzine micro emulsion preparation which is suitable for preventing and treating cranial vascular diseases. By utilizing the characteristics of nanoparticles and increasing the fat-soluble combination of the preparation, the brain targeting oral oil package oil chuanxiongzine micro emulsion preparation accelerates the medicineto permeate blood brain barrier, improves the selective enrichment of the medicine in the brain, provides higher medicine concentration in the brain, and obviously prolongs the residence time of the medicine in the brain, thus improving the prevention and treatment for corresponding brain diseases.
EP1267848B1 Dosing regimen comprising a farnesyl protein transferase inhibitor for the treatment of cancer This invention relates to a method of treatment and dosing regimen for treating mammalian tumors by the discontinuous administration of a farnesyl transferase inhibitor over an abbreviated one to five day dosing schedule.
US7815933 Pre-concentrate emulsion of a nitrogen oxide-releasing NSAID, a surfactant, and an oil or fat, for oral administration; forming an oil-in-water emulsion with gastrointestinal fluids; side- effect reduction; bioavailability; treating pain and inflammation The present invention claims and discloses a pharmaceutical composition suitable for oral administration, in form of an emulsion pre-concentrate, comprising (i) one or more NO-releasing NSAID(s); (ii) one or more surfactants, of which at least one is phospholipid; said composition forming an in-situ oil-in-water emulsion upon contact with gastrointestinal fluids. The composition may optionally also comprise an additional oil or semi-solid fat. Further, one or more short-chain alcohols can optionally be included in the composition. Also within the scope of the invention is a combination with a proton pump inhibitor. The pharmaceutical composition is useful in the treatment of pain and inflammation. Further within the scope of the invention is kit comprising a pharmaceutical composition according to the invention in a unit dosage form, in combination with a proton pump inhibitor, and said proton pump inhibitor is enteric coated.
CN103156874A Application of thorn wood bone glycosides B1 in antiviral drug of curing or preventing flu The invention relates to an application of thorn wood bone glycosides B1 in antiviral drug of curing or preventing flu. Influenza virus comprises influenza A virus and influenza B virus, and avian influenza virus which can infect a human body. The thorn wood bone glycosides B1 is taken as a single effective constituent by the antiviral drug to be manufactured to anti-influenza virus monotherapy, or the thorn wood bone glycosides B1 is taken as one of effective constituents to be manufactured to anti-influenza virus compound medicine, the weight content of the thorn wood bone glycosides B1 is 1-99%, the medicine is manufactured to any dosage forms of pharmaceutics, and the medicine is applied to prevent and cure infectious diseases caused by influenza virus.
WO2010018484A1 New uses of diisopropylamine derivatives The invention provides a diisopropylamine derivative selected from: (a) a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof; and (b) a pharmaceutically acceptable ester prodrug of the compound of formula I, and its pharmaceutically acceptable salts and solvates; for use in the treatment of stress urinary incontinence or mixed urinary incontinence. A preferred diisopropylamine derivative is fesoterodine, or a pharmaceutically acceptable salt thereof.
US20080015230 Heterocyclic derivatives and their use as therapeutic agents Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where y, G, K, L, M, W, V, R2, R3, R4, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
US20110301165 Method for treating and preventing arthritis Compounds represented by the formula 1: wherein each R individually is H, an aliphatic acyl group or an aromatic acyl group; A is selected from the group consisting of wherein X is selected from the group consisting of hydrogen, halo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro; are used to treat or prevent arthritis including rheumatoid arthritis.
US6916840 Spla2 inhibitors A novel class of benz[g]indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
US20110212184 Ultra Fine Dead Sea Mineral Compound and Method of Manufacture An ultra fine mineral compound and method of processing native Dead Sea minerals into this ultra fine mineral compound that can be used to manufacture all natural Dead Sea mineral compositions particularly compositions for use in bath and body products is disclosed. Even with the extreme ionic character of the Dead Sea minerals, the Dead Sea mineral compositions prepared remain in suspension creating a viable cosmetic preparation that can maintain adequate shelf life and provide a more pleasant feel for the consumer.
WO2009002425A3 Solubilized formulation of docetaxel without tween 80 Lyophilizates containing docetaxel and the use thereof in preparing concentrated liquid formulations, and ready to use formulations for injection, as well as such concentrates and ready to use formulations themselves are disclosed in which Tween surfactants are avoided so that hypersensitivity reactions to Tween surfactants can be avoided and docetaxel can be administered at higher doses and/or for longer periods of time and/or for additional treatment cycles.
WO2010072109A1 A sustained release system for tumor treating medicament A sustained release system for tumor treating medicament is disclosed. Said system contains degradable macromolecule vehicle, tumor treating agent and amifostine, in which the tumor treating agent comprises chemotherapy agent and one or more chemosensitizer, tumor targeting agent or lymph node tracer. Preferably, the weight ratio of chemotherapy agent to amifostine is 1: 0.001-20000. The sustained release system of present invention can be used for any tumor by changing different treating agent. The system of present invention is a new platform for any agent not only the current drugs but also the new drugs in the future.
CN101703773A Novel analgetic combined by two clinically-applied drugs and analgesic method The invention provides an analgetic combined by multiple ions channel blocker and aspartic acid receptor antagonist, is a new combination of the above two drugs, and realizes time difference of the two drug administration by a clinically-accepted sustained-release technology so as to result in obvious analgesic effect and be widely used in various chronic intractable pains in clinic. The novel compound analgetic has strong analgesic effect and endurable effect. The new combination which is old drugs to be newly used can lower usage dose of the single drug in clinic and can eliminate or delay the adverse effect of drug tolerance caused by the drug in clinic.
CN103189060A Compound useful for the treatment of nonsense-mutation-mediated diseases and pharmaceutical composition comprising said compound The present invention relates to the compound of formula (I) for use in the treatment of a nonsense-mutation-mediated genetic disease.
CN101919833A Application of aromatic compounds in preparing Caspase 3 inhibitor The invention discloses an application of aromatic compounds in preparing a Caspase 3 inhibitor which is used in preparing drugs for curing diseases such as neurodegenerative diseases, ischemic symptoms, sepsis and the like caused by Caspase 3 over expression, wherein the neurodegenerative diseases refer to Alzheimer's disease, parkinsonism or Huntington's disease; and the ischemic symptoms refer to stroke or myocardial infarction. The aromatic compounds can be obtained by fermenting and separating actinomycetes.
CN103694238A NO donor type matrine derivative and preparation method and medical application thereof The invention relates to the field of medical chemistry and pharmacotherapeutics, and particularly relates to an NO donor type matrine derivative and a preparation method thereof and application in pharmacy. The compounds have an anti-tumor effect and can be used for preparing anti-tumor medicines. The invention also relates to a preparation method of the compounds.
CN102697712A Disodium adenosine triphosphate injection and preparation method thereof The invention discloses a disodium adenosine triphosphate injection and a preparation method thereof. Only arginine is taken as a stabilizing agent. The preparation method comprises the following steps of: dissolving a prescription dose of disodium adenosine triphosphate into water for injection which is 20-30 DEG C and accounts for 60-80 percent of the total volume; stirring for dissolving; adding arginine into the solution; stirring uniformly till the pH value is 8.90-9.45; adding water for injection which is 20-30 DEG C to a full amount; degerming and filtering a liquid medicament; and filling according to theoretical content, plugging, capping and packaging. Only arginine is taken as an auxiliary material, is arginine which is necessary for human bodies, and is the source and standard of a medicinal auxiliary material; and when arginine is taken as a stabilizing agent, degradation of disodium adenosine triphosphate can be prevented effectively, the safety and effectiveness of clinical administration are enhanced, and the effective period of a medicament is prolonged.
US20100086582 Amorphous rotigotine transdermal system The present invention refers to a transdermal delivery device comprising a backing layer, an adhesive matrix layer comprising a supersaturated concentration of rotigotine substantially in amorphous form within the adhesive matrix, and a release liner. The present invention also refers to a method of preparing an adhesive matrix containing a supersaturated amount of rotigotine substantially in amorphous form. Further, the present invention refers to a method of stabilizing and a method of reestablishing the meta-stable amorphous-drug transdermal system during its manufacturing, storing, shipping and handling process.
EP2289488A2 Remedies for diseases to be applied to eye An agent for treating eye diseases contains sexual steroid hormone such as estrogen or its metabolites, its derivative, structural analogues thereof, estrogen acting substance or SERM or non-feminizing estrogen (non-hormonal estrogen) and has a form of eye drops or eye washes, etc.
WO2008028689A1 N-(1-phthalazin-1-ylpiperidin-4-yl)amides as ep2 receptor modulators The present invention relates to phthalazin-1-ylpiperidin-4-ylamides of the general formula (I), to processes for their preparation and to their use for producing pharmaceutical compositions for treatment of disorders and indications connected to the EP2 receptor.
US20060100238 4',7-Dihydroxyisoflavanone (phenyl)hydrazone; 4,7-Dihydroxyisoflavanone(4,7-dihydroxyisoflavanone)hydrazone; anticarcinogenic and antiinflammatory agents; cyclooxygenase inhibitor Aminated isoflavonoid synthesized by aminating the 4-keto group of isoflavanone and isoflavanone ring systems, pharmaceutical compositions containing same and uses thereof as therapeutic agents.
US20080214623 N-(2,2-Dimethylpropyl)-6-{3-fluoro-5-[(3-isoxazolylamino)carbonyl]-2-methylphenyl}-3-pyridinecarboxamide; inhibitors of p38 kinase The present invention relates to a novel compound, processes for its preparation, compositions comprising the same and its use in the treatment of condition or diseases mediated by p38 kinase activity.
US20070140975 Opioid formulations having reduced potential for abuse The invention provides opioid formulations having reduced potential for abuse, and having reduced potential for illegal sale and distribution. The opioid formulations of the invention comprise at least one opioid and a sustained release delivery system.
CN103181919A Stable ophthalmic formulations Disclosed herein are stable formulations suitabel for the treatment of glaucoma and ocular hypertension.
WO2007050034A1 Composition and method for the prevention, treatment and/or alleviation of an inflammatory disease A method for enhancing the clinical responsiveness to an anti- inflammatory therapy in a patient afflicted with an inflammatory condition, comprising administering an oligonucleotide having the sequence 5' -Xm-CG-Yn-3' in an effective amount to said patient, and wherein X is A, T, C or G; Y is A, T, C or G; m=l-40; n=l-40 and wherein at least one CG dinucleotide is unmethylated. The invention also encompasses the use of such an oligonucleotide for the manufacture of a medicament for enhancing steroid efficacy in the treatment of a patient afflicted with an inflammatory condition.
CN103373992A 1, 3, 4-Oxadiazole and pyridine (pyrazine) ring-containing acylhydrazone derivatives, preparation method and applications Provided are 1, 3, 4-oxadiazole and pyridine ring-containing acylhydrazone derivatives which are characterized by the following general formula:, wherein R is for, 1, 3, 4-oxadiazole and pyrazine ring-containing acylhydrazone derivatives which are characterized by the following general formula:, wherein R is for, and a preparation method. The 1, 3, 4-oxadiazole and pyridine (pyrazine) ring-containing acylhydrazone derivatives have obvious inhibiting effects on human lung cancer cells A549, human liver cancer cells HepG2, human breast cancer cells MCF7 and human stomach cancer cells SGC7901, so the 1, 3, 4-oxadiazole and pyridine (pyrazine) ring-containing acylhydrazone derivatives can be applied to preparation of anti-cancer drugs.
CN1839869A Use of molo glycoside in alpha-glucosaccharase inhibitor The invention provides a novel Moluo glycoside with natural source as an alpha-glucosidase depressant, and discloses a process for preparing the Moluo glycoside from natural plants such as Patrinia villosa Juss. and cornus officinalis. The invention also discloses the use of Muluo in treating diabetes.
EP1699398A2 Enhancement of immune responses The present invention provides methods for enhancing the immune responses induced by IRM compounds. Generally, the methods include administering a cytokine receptor agonist or a cytokine inducer prior to administering an IRM compound to a cell population.
CN101239060A Medicinal composition for preventing and controlling poultry intestinal canal disease and preparation thereof The invention relates to a medicine compound for curing and preventing the inflammatory bowel diseases suffered by the poultry, and the method for preparing such medicine compound. The ingredients and the weight percentages of the ingredients are respectively 1 to 10 percent enrofloxacin, 1 to 10 percent lincomycin hydrochloride, 1 to 10 percent latent solvent, and 100 percent other additive accessories. The preparation method is mixing and fully agitating the 1 to 10 percent enrofloxacin, the 1 to 10 percent lincomycin hydrochloride, the 1 to 10 percent latent solvent, and the other additive accessories, which are crushed and screened, according to the weight percentages, so a medicine compound for curing and preventing the inflammatory bowel diseases suffered by the poultry comes into being. The formulation of the invention is reasonable and scientific, the use is convenient, and the function of double sterilization is achieved. The enrofloxacin can effectively restrict the compounding and duplication of DNA so as to kill the bacteria, through the action onto the A subunit of the DNA gyrase. The lincomycin hydrochloride can kill the bacteria through restricting the compounding to the protein of the cells of the bacteria. Both functions together make the sterilization quick and highly efficient, and the medicine compound applicable for large-scale production and popularization.
WO2014021667A1 Composition for treating cancer associated with hpv infection The present invention relates to a composition for preventing or treating diseases associated with human papillomavirus (HPV), and more specifically, cancer associated with HPV, and even more specifically, cervical cancer. The nucleotide sequence of the present invention, the sequence in which the base thereof is modified, and a specific combination thereof can be useful in a composition for effectively treating diseases associated with HPV infection by greatly inhibiting the expression of the E6/E7 gene of HPV type 16 or 18.
US20080317667 Compositions and methods for inhibiting growth of smad4-deficient cancers The present invention is in the fields of cell biology, immunology and oncology. The invention relates to the discovery that there is a relationship between the expression levels of the tumor suppressor gene smad4 (also known as dpc4) and integrin αvβ6, and the responsiveness of patient populations to αvβ6-active compounds and compositions (e.g., antibodies and other ligands that bind αvβ6), particularly in cancer cells from such patient populations, more particularly on carcinomas such as pancreatic carcinomas. The invention thus provides methods for determining the responsiveness of tumor cells (particularly those from pancreatic tumors) to such αvβ6-active compounds and compositions by examining the expression of αvβ6 and smad4 by the tumor cells, as well as methods of diagnosis and treatment/prevention of tumor progression using ligands, including antibodies and small molecule drugs, that bind to integrin αvβ6 on the surfaces of tumor cells and/or that block one or more components of the TGF-β pathway, particularly in smad4-deficient tumor cells.
EP1021084B1 Solution and process for resuscitation and reparation of ischemically damaged tissue The invenetion discloses a process and resuscitation solution for inducing repair of ischemically damaged organs and tissues, to the degree that impairment of function can be reversed; and preventing further tissue damage during restoration of the circulation of the treated organ or tissue. The process comprises flushing the organ with the resuscitation solution according to the present invention at a warm temperature of about 28 °C to about 37 °C to remove accumulated blood and acidotic products from blood flow deprivation; and perfusing the flushed organ or tissue with the resuscitation solution, wherein the solution contains a novel combination of components to provide for (i) dilating of the blood vessels within the organ or tissue, (ii) reestablishing organ or tissue function by supplying trophic factors, (iii) restoring cellular integrity and function to the ischemically damaged organ or tissue, and (iv) reestablishing oxidative metabolism by readapting the ischemically damaged organ or tissue, surviving by anaerobic respiration, to an oxygenated resuscitation solution.
CN102499322A Novel health-care food or drug with function of improving memory The invention provides a novel health-care food or drug with the function of improving memory. The health-care food or drug can reduce the content of acetylcholinesterase, further reduce the decomposition of acetylcholine, improve the content of BDNF (brain derived neurophic factor), and improve memory. Besides, even through the food or drug is ate by healthy people that have no memory barriers, the inhabitation of the acetylcholinesterase as well as BDNF can improve memory; mild cognitive impairment resulting from declining memory of health people can be further effectively prevented, and senile dementia can be further prevented.
CA2574904C Antiretroviral enantiomeric nucleotide analogs Resolved enantiomers of formulae (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.
WO2013004740A1 Anticonvulsant activity of turmeric oil and bisabolene sesquiterpenoids The present invention relates to the anticonvulsant activity of turmeric oil and its volatile bisabolene sesquiterpenoids ar- turmerone, α-turmerone, β-turmerone (curlone) and α- atlantone, as an anticonvulsant agent for the treatment of epilepsy and/or as therapeutic agents for the treatment of disorders of the central nervous system, including tremor, pain, mood disorders (including depression, bipolar disorder, attention deficit-hyperactivity disorder, and schizophrenia), and neurodegenerative diseases.
CA2250309C Steroids as neurochemical initiators of change in human blood levels of lh or fsh The invention relates to a method of altering the blood levels of LH or FSH in an individual. The method comprises nasally administering a steroid which is a human vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.
US20050100563 Tin oxyfluoride or other transition metal halides in aqueous solution produce mild hydrohalo acid; topical application to affected skin and nails The invention is an aqueous or aqueous/alcoholic solution of a transition metal halide, a transition metal oxyhalide, and/or the hydrolysis products thereof as an antifungal composition and method of treating fungal infections therewith. The composition may be used for humans and/or animals in need of topical antifungal treatment. The invention is particularly adapted to use for onychomycotic infections. The transition metal is selected from the groups consisting of copper, zinc, gallium, germanium, silver, tin and mixtures thereof (mixed metal compounds such as [SnZnF4]), which can be in any oxidation state (other than that of the totally reduced metal). The halide is selected from the group consisting of fluorine, chlorine, bromine, iodide, and mixtures thereof (a mixed halide such as in [SnF2Cl]−). The transition metal compounds may also be mixed oxides and halides such as in stannous oxyfluoride (Sn4OF6) or stannic oxyfluoride (SnOF2). Since the compounds are in solution, they may also exist as hydrolysis products of any of the foregoing. The compositions have a pH of about 2 to about 4.
US8592383 Cycloalkyl-fused tetrahydroquinolines as CRTH2 receptor modulators The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
EP2193127A1 Benzothiazole compounds The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival.
US20110124587 Pure Rebaudioside A The invention provides a high throughput, high purity, high yield system and method of isolating and purifying rebaudioside A (“Reb A”), with acceptable water solubility for all commercial uses, from commercially available Stevia rebaudiana starting material. The invention also provides a means of maximizing yields of 99+% purity Reb A based on the attributes of a given batch of Stevia starting material. The purity of the Reb A final product, up to 99+% purity, can be selected based on a starting material assay.
CN1654040A Novel medical uses of perennial sowthistle and preparing method for intermediate thereof The present invention is the new application of denticulate ixeris herb in treating cardiac and cerebral vascular diseases and leukaemia and the preparation process of its medicinal intermediate. The extract of denticulate ixeris herb contains sesquiterpene lactone and phenoloid and thus has the functions of increasing blood flow rate of coronary artery, improving myocardial circulation, inhibiting thrombocyte aggregation, raising the activity of plasmin, etc. The preparation process of the medicinal intermediate includes water or alcohol extraction and chromatographic purification in combined macroporous resin and polyamide column. The intermediate has total content of total flavone and total lactone of 60-95 %.
WO2010126030A1 Spiroimidazolone derivative Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims.)
US20130052276 Method for Making an Antimicrobial Material from One-dimensional Nanometer Silver that Does Not Accumulate in a Human Body Disclosed is a method for making an antimicrobial material from 1D nanometer silver that does not accumulate in a human body. At first, 1D nanometer silver is mixed in hydrophilic solution to produce 1D nanometer silver solution. Then, adhesive is blended in the 1D nanometer silver solution to produce the antimicrobial material. The antimicrobial material may be used in antimicrobial liquid, antimicrobial dressing or antimicrobial composite. Human skin can easily block the 1D nanometer silver. Therefore, the 1D nanometer silver does not enter or accumulate in the human body. Yet, the antimicrobial material exhibits a high bactericidal rate.
US20120252898 Method of producing a stabilized naturally occuring hydroxycitric acid (hca) from garcinia indica fruit A method of producing a stabilized naturally occurring hydroxycitric acid is provided. In one embodiment, the method comprises combining an aqueous liquid with Garcinia indica fruit to provide an aqueous extract containing hydroxycitric acid and mixing the aqueous extract containing hydroxycitric acid with a liquid quaternizing agent wherein the aqueous liquid comprises at least 8 mg/ml anthocyanin per 100 ml of liquid.
CN101697971A Rehabilitation therapy method for lung cancer The invention provides a rehabilitation therapy method for lung cancer, comprising medicament treatment and nutrient treatment. The method adopts vincristine (VCR), cyclophosphamide (CTX) and carboplatin (CBP) as principle proposal chemotherapy, and simultaneously adopts a method by using bioactive modifier and venous alimentation treatment, thereby improving the immune function of bodies, and improving living quality. The method has good curative effect, can tolerate toxic and side reactions in the chemotherapy, has good clinical application value, and is easy for popularization.
WO2011012659A3 Diethyl 4-(4-fluorobenzylamino)-1,2-phenylenedicarbamate, and salts thereof Disclosed are diethyl 4-(4-fluorobenzylamino)-l,2-phenylenedicarbamate (IV) and salts thereof, which are useful as reference markers and reference standards for analyzing samples comprising retigabine or salts thereof. Also disclosed is a process for preparing a compound (IV) and salts thereof.
WO2012168733A1 Substituted 8 - amino - imidazo [1, 2-a] pyrazines as antibacterial agents The present invention relates to substituted imidazofi,2-a]pyrazines of Formula (I) and their use as antibacterial agents.
CN102847021A Enema for treating ulcerative colitis and preparation method thereof The invention discloses an enema for treating ulcerative colitis. Bulk drugs for the enema comprise, by weight, 10 to 20 parts of pasque flower, 10 to 20 parts of Chinese yam, 10 to 20 parts of common bletilla, 10 to 20 parts of root of large-flowered skullcap, 10 to 20 parts of dahurian angelica root, 10 to 20 parts of mutmeg, 10 to 20 parts of red sage root, 10 to 20 parts of glabrous greenbrier rhizome, 10 to 20 parts of garden burnet, 10 to 20 parts of milkvetch root, 10 to 20 parts of Chinese angelica, 10 to 20 parts of coptis, 10 to 20 parts of heydyotis, 10 to 20 parts of red halloysite, 10 to 20 parts of sophora flower, 10 to 20 parts of Chinese gall, 10 to 20 parts of garlic, 10 to 20 parts of pomegranate rind and 10 to 20 parts of atractylodes rhizome. The enema provided by the invention enables medicines to directly reach a focus, can be used for local flushing and can check diarrhea, diminish inflammation, resolve tetany, relieve pains, improve local blood circulation and metabolism, enhance immunity of intestinal tracts and promote healing of ulcers. With an anorectal therapy, the medicines can reach a focus after administration and medicines act on the focus in high concentration, which is beneficial for the medicines to take effect, and thus, the purposes of eliminating pathogenic factors and repairing injured tissue are achieved.
CN103415290A Compounds useful for treating AIDS The present invention relates to compound (I) for use as an agent for preventing, inhibiting or treating AIDS. The present invention further relates to compounds of formula (I), wherein X is CR0 or N; R0, R1, R2, R3, R4, R7 and R8 independently represent a hydrogen atom, a halogen atom or a group chosen among a (C1-C5)alkyl group, a (C3-C6)cycloalkyl group, a (C1-C5)fluoroalkyl group, a (C1-C5)alkoxy group, a (C1-C5)fluoroalkoxy group, a -CN group, a -COORa group, a -NO2 group, a -NRaRb group, a -NRa-SO2-NRaRb group, a -NRaSO2Ra group, a -NRa-C(=0)-Ra group, a -NRa-C(=0)-NRaRb group, a -SO2-NRaRb group, a -SO3H group, a -OH group, a -O-SO2-ORc group, a -O-P(=O)-(ORc)(ORd) group, a -O-CH2-COORc group can further be a group chosen among: (IIa), (IIIa), R5 represents a hydrogen atom, a (CrC5)alkyl group or a (C3-C6)cycloalkyl group; R10 is a hydrogen atom or a chlorine atom, and R11 is a hydrogen atom or a (C1-C4)alkyl group or anyone of its pharmaceutically acceptable salts.
CN101371909A Medicine for treating carcinoma of stomach and preparation method thereof The invention relates to a medicament for treating gastric cancer, and the medicament is composed of swordlike atractylodes rhizome, twotooth achyranthes root, alum, trogopterus dung, eucommia bark, pine nut, cold food flour and liquor. The invention further relates to a preparation method of the medicament for treating gastric cancer. The medicament has the advantages of scientific and reasonable formula, good efficacy, less toxicity or side effects, and the like.
US20100129438 Methods and Compositions for the Treatment and Prevention of HIV Infection Using TRIM5ALPHA The invention provides novel TRIM polypeptides, proteins, and nucleic acid molecules. In addition to isolated, full-length TRIM proteins, the invention further provides isolated TRIM fusion proteins, antigenic peptides and anti-TRIM antibodies. The invention also provides TRIM nucleic acid molecules, recombinant expression vectors containing a nucleic acid molecule of the invention, host cells into which the expression vectors have been introduced and non-human transgenic animals in which an TRIM gene has been introduced or disrupted. The present invention also provides methods and compositions for the diagnosis and treatment of viral infection and/or replication, e.g., HIV infection. The invention further provides methods for identifying a compound capable of treating or preventing viral infection and/or replication, e.g., HIV infection and AIDS. In addition, the invention provides a method for treating a subject having a viral infection and/or replication, e.g., HIV infection using the modulators of the invention.
US20080058286 Antidiabetic agents, metabolism disorders, cardiovascular disorders, antiinflammatory agents, fertility, muscular disorders, obesity; marine phosphatide This invention disclose novel uses of omega-3 rich phospholipids for treating diabetes type II, metabolic syndrome, sustained ventricular tachycardia and inflammatory disease. In addition to improving fertility in asthenozoospermic males. The invention also discloses the use of omega-3 rich phospholipids in healthy subject for improving physical endurances, reducing delayed onset muscle soreness as well as preventing obesity.
WO2012160187A1 Amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives and their medical use The present invention relates to amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives, in particular the compounds of formula 1, 2, 3, 4, 5 or 6, and their medical use, including their use in the treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder.
WO2011057477A1 Tetrapeptide analogs, preparation method and use thereof The present invention discloses second mitochondria-derived activator of caspases (Smac) analogs of formula I or their pharmaceutically acceptable salts and the preparation method thereof. The invention also discloses the use of compound of formula I as anticancer agent by inducing tumor apoptosis, wherein R1 and R2 are defined by the description of the invention.
WO2014072493A1 Pharmaceutical combination comprising a b-raf inhibitor and a histone deacetylase inhibitor and their use in the treatment of proliferative diseases A pharmaceutical combination comprising (a) a B-Raf inhibitor and (b) a historic deacetylase inhibitor; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.
EP1684751A1 Use of 1-thia-dibenzo e,h azulenes for the manufacture of pharmaceutical formulations for the treatment and prevention of central nervous system diseases and disorders The present invention relates to the use of derivatives from the group of 1-thia-3-azadibenzo[e,h]azulenes and of their pharmaceutically acceptable salts and solvates for the manufacture of a pharmaceutical formulation for the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other neurotransmitters.
CN102702377A Termitomyces albuminosus polysaccharide separation and purification method and injection thereof The invention discloses a termitomyces albuminosus polysaccharide separation and purification method, which comprises the following steps of: extracting at ultrasonic power of 20 kHz, temperature of 80 DEG C and material-liquid ratio of 1:20 for 40 minutes by using an ultrasonic method; extracting twice in total to obtain polysaccharide crude extract; preparing the polysaccharide crude extract into a solution with concentration of 20 percent; freezing at -20 DEG C; slowly melting at room temperature; centrifuging at 3,000 r/min for 10 minutes to remove aggregative deposit; repeatedly freeze-thawing for five times; mixing the freeze-thawed polysaccharide solution and a Sevage reagent according to a proportion of 4:1; fully oscillating for 30 minutes; centrifuging at 2,000 r/min for 10 minutes, wherein the under layer white flocculent precipitate is a protein layer; and collecting the upper layer polysaccharide solution. The experimental result proves that the humoral immunity and the cellular immunity capacity of an experimental animal can be obviously improved with a certain dose of TAP (Transporter Associated with antigen Processing), and the effect is superior to that of the same dose of APS (Astragalus polysaccharide).
US20100048565 Benzimidazole derivatives Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives.
CN103735655A Medicinal liquor for treating dysmenorrhoea The invention relates to a nutritional buccal tablet for treating dysmenorrhoea. The nutritional buccal tablet is prepared by immersing 10-15 g of Chinese angelica, 10-15 g of radix paeoniae alba, 8-10 g of radix codonopsis, 3-5 g of red date, 8-15 g of walnut kernels and 10-15 g of xylitol in 100-200 mL of Chinese liquor for 20-30 days. The medicinal liquor for treating dysmenorrhoea is capable of activating blood, tonifying blood, dredging and moistening blood vessel, regulating menstruation and treating dysmenorrhoea, and also is abundant in nutrition, good in product mouthfeel, convenient to use and carry, low in cost. The medicine provided by the invention has the characteristics of being good in curative effect, fast in effectiviness, simple in preparation, convenient to take, free of toxic and side effects, convenient for material drawing and low in price, and is mainly used to treat and alleviate dysmenorrhoea.
EP1087951B1 Carbon substituted aminothiazole inhibitors of cyclin dependent kinases The compounds of formula (I) are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, and cardiovascular disease.
CN101637456B Suspension powder injection of cefamandole nafate and new application thereof The invention relates to suspension powder injection of cefamandole nafate and a preparation method thereof and further relates to new application of the injection in treating acute suppurative cholangitis. The frozen-dried suspension powder injection comprises the following components in parts by weight: 1 part of cefamandole nafate, 1.5-12 parts of surfactant and 2-15 parts of frozen-dried supporting agents.
WO2009109983A1 Thieno[2,3-d]-pyrimidine-4(3h)-one compounds with antifungal properties and process thereof The present invention discloses novel compounds of the Formula (1), containing thieno- [2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.
US20060258602 Site-specific gene conversion promoter and gene therapeutic It is intended to provide a preparation whereby an oligonucleotide is efficiently transferred into a cell and the localization thereof in nucleus is promoted, a preparation for facilitating the conversion of the base sequence of a target genomic gene, and a preparation for gene therapy. Namely, a preparation for facilitating site-specific gene conversion which comprises at least a collagen and an oligonucleotide for gene conversion; a preparation for site-specific gene therapy which comprises at least a collagen and an oligonucleotide for gene conversion; a method of arbitrarily converting a specific base on a genomic gene in the nucleus of a cell which comprises bringing the above-described preparation for facilitating gene conversion into contact with the cell; and an preparation for facilitating oligonucleotide intranuclear localization which comprises at least a collagen and an oligonucleoitde.
CN101596166B Aspirin enteric-coated pellet The invention discloses an aspirin enteric-coated pellet which comprises the following components in percentage by weight from inside to outside: 5-22 blank core pellet, 55-75 medicinal layer consisting of aspirin and medicinal excipients and 20-35 enteric-coated layer. The invention also discloses a method for preparing the aspirin enteric-coated pellet and an aspirin enteric-coated capsule containing the aspirin enteric-coated pellets. The aspirin enteric-coated capsule has the advantages of good stability, small stimulation, steady blood concentration, high bioavailability, and the like.
CN202236438U Externally-applied plaster for treating pharyngitis The utility model discloses externally-applied plaster for treating pharyngitis. The externally-applied plaster is characterized in that one side of a non-woven fabric basal body is coated with colloidal matter; a protecting film matched with the non-woven fabric basal body is arranged on the side, which is coated with colloidal matter, of the non-woven fabric basal body; and a drug layer is arranged between the protecting film and the non-woven fabric basal body. The externally-applied plaster for treating pharyngitis takes effect quickly, releases slowly, acts for a long time, is safe and convenient to use, and can be directly applied to the cervical vertebra and the Taotao.
WO2010047756A1 Oral dosage forms including an antiplatelet agents and an enterically coated acid inhibitor The present disclosure provides oral dosage forms comprising an antiplatelet agent and an enterically coated acid inhibitor, as well as methods of treating subjects with an antiplatelet agent and an enterically coated acid inhibitor.
CN102462791A Medicine for oral administration for treating fracture The invention discloses a medicine for oral administration for treating fracture, which comprises the following bulk drugs by weight part: 1-3 parts of rhizoma ligustici wallichii, 5-10 parts of dragons blood, 1-2 parts of red sage root, 14-18 parts of radix pseudoginseng, 5-9 parts of Radix Rehmanniae Preparata, 3-8 parts of cortex eucommiae, 2-4 parts of bidentate achyranthes, 10-12 parts of radix dipsaci, 10-15 parts of malaytea scurfpea, 10-15 parts of frankincense, 2-5 parts of Siphonostegia chinensis, 2-4 parts of ground beetle, 1-2 parts of hematoxylon, 10-15 parts of premna fulva craib, 12-18 parts of glabrous sarcandra herb, 3-6 parts of pyrite, 1-3 parts of corydalis tuber, 3-6 parts of root of Japanese banana and 2-4 parts of creeping woodsorrel herb. The medicine for oral administration for treating fracture has the functions of joining the tendon and bone, strengthening the tendon and bone, activating blood and dissolving stasis, warming channels and freeing networks vessels, smoothing sinews and dissipating binds and the like, and has the advantages of filling qi to run blood, generating blood and nourishing the blood, tonifying liver and invigorating qi, and has the merits of no toxic and side effect, convenient administration, substantial curative effect and fast effectiveness, wherein the curative effect for fracture is as high as 99%.
WO2011001028A1 A bioactive glass for use in conditions relating to bone infections The present invention relates to a bioactive glass having the composition of SiO2 44-65 wt-% of the final total weight, Na2O 5-26 wt-% of the final total weight, CaO 10-25 wt-% of the final total weight, K2O 0-1 5 wt-% of the final total weight, MgO 0-6 wt-% of the final total weight, B2O3 0-4 wt-% of the final total weight, and P2O5 0-7 wt-% of the final total weight, for use in the long- and short-term prevention and/or treatment of conditions relating to or caused by bone infections, provided that the total amount of Na2O and K2O is 10-30 wt-% of the final total weight, and that any source of oxygen capable of releasing oxygen in the form of molecular oxygen or reactive oxygen species, is absent.
US7138406 Antiinflammatory agents; antiallergens; vision defects; anticancer agents; gastrointestinal disorders The present invention provides compounds of the formula wherein A is of the formula and X, Y, n, R1–R25 are as described in the specification which are modulators of the glucocorticoid receptor and are thus useful for the treatment of animals requiring glucocorticoid receptor agonist therapy. Glucocorticoid receptor modulators are useful in the treatment of certain inflammatory conditions.
CN101288686B Health preparation for increasing bone density and preparation method thereof The invention relates to a health preparation for increasing bone density. Calcium carbonate and other calcium compounds, rhizoma drynariae, eucommia bark (or eucommia bark leaf) and CPP (or vitamin D3) are taken as main raw materials, and the preparation is prepared according to a certain weight ratio. The invention combines calcium carbonate and other calcium compounds, CPP and other calcium-absorption accelerant, rhizoma drynariae, eucommia bark (or eucommia bark leaf) and other medicinal herbs together to produce the synergistic effect, thus effectively promoting human calcium absorption and improving bone status. The product has the efficacy of benefiting liver and kidney, strengthening bones, replenishing calcium source and increasing bone density.
CN102525908A Carbazochrome sodium sulfonate pharmaceutical composition and preparation method thereof The invention relates to a carbazochrome sodium sulfonate pharmaceutical composition, which is prepared from the following components in part by weight: 20-80 parts of carbazochrome sodium sulfonate, 40-120 parts of lactose, 3-6 parts of poloxamer 188, 1-4 parts of glutathione, 0.05-0.2 parts of disodium edetate and 2000 parts of water for injection. The preparation of the carbazochrome sodium sulfonate pharmaceutical composition is lyophilized powder for injection or water needle injection. According to the invention, lactose, poloxamer 188, glutathione and disodium edetate are used as adjuvants, wherein mannitol is used as an excipient, poloxamer is used as a co-solvent and a stabilizer, and glutathione and disodium edetate are used as an antioxidant and a metal-chelator. The combined use of these adjuvants and the composition formed of carbazochrome sodium sulfonate take remarkable effects on improving appearance, redissolution, stability and other indicators of medicines.
US7255881 For therapy of undesirable skin conditions Metal-containing materials, as well as their preparation and use are disclosed. The metal-containing material can be, for example, an antimicrobial material, an anti-biofilm material, an antibacterial material, an anti-inflammatory material, an anti-fungal material, an anti-viral material, an anti-cancer material, a pro-apoptosis material, anti-proliferative, MMP modulating material, an atomically disordered, crystalline material, and/or a nanocrystalline material. In certain embodiments, the metal-containing material is an atomically disordered, nanocrystalline silver-containing material.
CN101284058A Sobering-up agent and its preparation process The invention discloses an anti-hangover preparation and a preparation method thereof. The acer truncatum leaf extract is obtained by extracting with alcohol, concentrating, adsorbing with macroporous resin, eluting, concentrating, drying and pulverizing of the acer truncatum leaves; the raisin tree seed extract is obtained by extracting with alcohol, concentrating, drying and pulverizing of the raisin tree seeds; mixing the acer truncatum leaf extract, the raisin tree seed extract, kudzu root powder, hawthorn power and VB6 as the inventive active components of the anti-hangover preparation; and preparing into oral preparation in a conventional method. The anti-hangover preparation combines the medicinal and edible plants, has accurate and balance contents and no toxicity, and can be conveniently edible for a long time. The preparation is effective in resisting hangover, clearing away heat and toxic material, protecting the liver, enhancing microcirculation in vivo, reducing headache and dizziness after drunk, remarkably reducing over-high blood lipid concentration in the blood, and can be used for prevention and auxiliary treatment of diseases such as arteriosclerosis, thrombosis, coronary heart disease, etc.
CN102532341A Extraction method and application of chroogomphus rutilus polysaccharide The invention discloses an extraction method and application of chroogomphus rutilus polysaccharide with anti-motion sickness effects. The polysaccharide takes chroogomphus rutilus as a raw material, and is prepared by a water extraction and alcohol precipitation method. The chroogomphus rutilus polysaccharide is used for prevention and treatment of motion sickness, and the results show that very good anti-motion sickness effects can be provided when 200mg/kg of chroogomphus rutilus polysaccharide is given to the stomach by behavioral experiments and hormone level tests. The motion sickness symptoms such as visceral discomfort, incontinence, piloerection and tremor can be obviously reduced, and the level of 5-HT in serum can be reduced, and the motilin level is improved; and most importantly, rats are in good spirits, has no low spirits and other side effect symptoms. The 200mg/kg of chroogomphus rutilus polysaccharide is an ideal dose for the polysaccharide anti-motion sickness. The extraction method provides a novel material and a reference dose for further development of novel anti-motion sickness drugs with efficient, non-toxic and non-side effects.
US20100087504 Use of Diindolylmethane (DIM) Compounds and Derivatives as Neuroprotective Agents Presented herein are diindolylmethane derivative compounds useful for the prevention and or treatment of neurological conditions, including neurological conditions related to neuroinflammation. One such neurological condition is Parkinson's disease.
CN101402565A Halogenated 2-(a-hydroxyl pentyl) benzoate, production method and uses thereof The invention discloses a halogen substituted 2-(a-hydroxyl amyl) benzoate compound, a preparation method and medicinal application thereof, which belong to the technical field of organic chemical synthesis. The structural formula of the compound which is showed as above has an antimer structure, wherein represents a halogen atom; n is equal to 1 to 3; and M represents a univalent metallic ion or a bivalent metallic ion or a trivalent metallic ion or an organic base. The compound has the advantages of better activity on preventing and treating cardio-cerebral ischemia diseases, improving cardio-cerebral circulation disturbance and resisting thrombus, and the like.
US20100305091 PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES Compounds of the following formula (I) are inhibitors of microtubule affinity regulating kinase, and hence find use in the treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.
US7307176 Inclusion complex of taxol with 2-hydroxypropyl-beta-cyclodextrin The present invention relates to a method for producing a 2-hydroxypropyl-beta-cyclodextrin inclusion complex of taxol, said 2-hydroxypropyl-beta-cyclodextrin having a degree of substitution of 0.4 to about 0.9, wherein the method comprises admixing the 2-hydroxypropyl-beta-cyclodextrin with taxol at a molar ratio of 1-1000 times with respect to taxol. A second aspect of the invention relates to a method for improving the solubility of taxol, said method comprising: (i) dissolving taxol in ethanol; (ii) dissolving 2-hydroxypropyl-beta-cyclodextrin, having a degree of substitution of 0.4 to about 0.9, in water; (iii) admixing the solution from step (i) with the solution from step (ii) and stirring, shaking or heating. A third aspect of the invention provides a 2-hydroxypropyl-beta-cyclodextrin inclusion complex of taxol, wherein said 2-hydroxypropyl-beta-cyclodextrine has a degree of substitution of 0.4 to about 0.9.
CN102068449A Novel use of rutin The invention belongs to the field of medicines and relates to novel use of rutin, namely use of the rutin in preparing medicines for treatment and liver protection. Pharmaceutical experiments prove that: the rutin can effectively relieve low-temperature preservation and reperfusion injury of a liver transplant, protects donor liver and is taken 0.5 to 2mg per day.
US20080220093 Methods for production of the oxidized glutathione composite with cis-diamminedichloroplatinum and pharmaceutical compositions based thereof regulating metabolism, proliferation, differentiation and apoptotic mechanisms for normal and transformed cells The present invention relates to a composite for the treatment of a variety of medical conditions, the composite comprising an oxidized gluthathione-based compound, which has a disulfide bond, and a metal material, in particular where the metal is either platinum or palladium. The oxidized glutathione-based compound and metal material can be present in a ratio of 3000 to 1 and preferably 1000 to 1. The oxidized glutathione-based compound can be oxidized glutathione itself or salts or derivatives. A feature of the invention is that the composite has a more stabilized disulfide bond than the oxidized glutathione-based compound itself. Methods for preparing the composite are provided, such methods being beneficial in that the composite is provided in high yields and at high purity. Methods for treating various medical conditions with the composites of the present invention are also disclosed.
CN102659904A Preparation method for hederagenin and salts thereof The invention discloses a preparation method for hederagenin and the salts thereof, comprising the following steps of: extracting Dipsacus asperoides via ethanol, recovering a solvent from the extracted solution at a reduced pressure, purifying via macroporous adsorption resin or extracting and purifying via n-butyl alcohol to obtain Dipsacus asperoides total saponin, performing alkaline hydrolysis and acid hydrolysis on the Dipsacus asperoides total saponin, and then crystallizing or refining via the macroporous adsorption resin to obtain high-purity hederagenin, and reacting the hederagenin with alkali to prepare the salts of the hederagenin finally. According to the invention, the raw materials are abundant in the source and low in price; the whole preparation process is free from the use of toxic reagents, safe and low-toxicity; the preparation process is simple, high in separation and purification efficiency, greatly improved in the purity and productivity of the products, suitable for industrialized production, easy to popularize and apply, and remarkable in pharmacologic action; and a new medicine source is provided for treatment and research on hyperlipidemia.
WO2008079721A1 Alpha-2 receptor pan agonist and serotonin-norepinephrine reuptake inhibitor compositions for treating chronic pain Disclosed herein is a pharmaceutical composition comprising a serotonin- norepinephrine reuptake inhibitor and a pan-alpha-2 receptor agonist. The composition is effective for treating chronic pain, and methods of treating pain using the composition and compounds comprising it are also disclosed.
WO2014146493A1 Acyclic cyanoethylpyrazolo pyridones as janus kinase inhibitors The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
US20050272791 Lung melanoma metastasis, rheumatoid arthritis, 1-isopropylsulfonyl-2-amino-6-(2-(2,6-difluorophenyl)-5-(phenyl)-imidazol-4-yl)-benzimidazole The present invention provides kinase inhibitors of Formula I: wherein W represents inter alia imidazol, oxazol, pyrazol, thiazol as triazol, which are substituted by phenyl or thienyl. The disclosed compounds inhibit p-38 kinase and are useful in the treatment of metastasis or rheumatoid arthritis.
US20080051462 Methods for treating genetically-defined proliferative disorders with HSP90 inhibitors The invention relates generally to methods of treating cell proliferative diseases with HSP90 inhibitors and, depending on the specific aspect and embodiment(s) claimed, to the treatment of proliferative diseases that are associated with fusion proteins, e.g., berab1, or mutant proteins or cellular protein isoforms, e.g., mutant forms of p53.
EP1539687A1 Substituted glycine derivatives for use as medicaments The compounds of formula (I) are substituted glycine derivatives useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, sleep disorders, visceral pain disorders and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included. Formula (I) wherein R' is hydroxycarbonyl, a carboxylic acid biostere or prodrug thereof; R3, R3a, R2 and R2a are independently selected from H, C1-C6 alkyl, and Cl-C6 alkoxy Cl-C6 alkyl.
EP1406888B1 Substituted y-lactone compounds serving as nmda antagonists The invention relates to substituted η-lactone compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.
EP1221445B1 Pentacyclic taxane compounds Novel Taxol derivatives having various substituents as represented by general formula (I) and being usable as antitumor compounds which can be orally administered.
CN102697666A Cyclodextrin salicylic acid inclusion complex aqueous solution, as well as preparation method and application thereof The invention belongs to the technical field of health care and in particular relates to a cyclodextrin salicylic acid inclusion complex aqueous solution, as well as a preparation method and application thereof. The cyclodextrin salicylic acid inclusion complex aqueous solution is prepared by mixing cyclodextrin aqueous solution and salicylic acid aqueous solution according to a certain molar ratio and standing at the temperature of 0 to 100 DEG C for more than one hour. The prepared cyclodextrin salicylic acid inclusion complex aqueous solution can be used for preparing cosmetics or medicines directly contacted with skin, such as anti-acne cream, toner, cleanser and shampoo. The cyclodextrin salicylic acid inclusion complex aqueous solution can adjust the release speed of the salicylic acid on the surface of skin, reduce the irritation and the toxic or side effect of the salicylic acid and reduce the irritation of the overrich salicylic acid on the skin. The invention has readily available material, a simple and convenient production process and achieves good economic benefit.
EP2579862A1 Pharmaceutical composition with olive extract (hydroxytyrosol) and hop extract (xanthohumol) for intranasal application The invention relates to a pharmaceutical composition containing hydroxytyrosol (olive extract) and xanthohumol (hop extract) as active substances for intranasal application, in particular in the form of a nasal spray for the prophylactic and/or curative treatment of colds.
WO2007144985A1 Use of rpn2 gene expression inhibitor Disclosed is use of an RPN2 gene expression inhibitor as a cancer cell proliferation inhibitor. If required, the cancer cell proliferation inhibitor may further contain an agent having an anti-cancer activity. If required, the cancer cell proliferation inhibitor may be administered together with atelocollagen. Also disclosed is an anti-cancer agent comprising the cancer cell proliferation inhibitor.
CN103040824A Signal channel inhibiting agent as well as preparation method and application thereof The invention belongs to the field of a chemical medical technology and particularly relates to a signal channel inhibiting agent as well as a preparation method and an application thereof. The signal channel inhibiting agent is characterized in that the structure is shown as the formula I (which is as shown in the description); and an experiment shows that the IC50 (half maximal inhibitory concentration) of the signal channel inhibiting agent to a Hedgehog signal channel is in a range of 30 nanomoles to 10 micromoles, and the signal channel inhibiting agent can be used for preparing a medicine for treating diseases which are related to abnormal activation of the Hedgehog signal channel.
CN102319262A 5% glucose child nutrient solution and preparation method thereof The invention belongs to the technical field of child nutriment, and particularly relates to a 5% glucose child nutrient solution and a preparation method thereof. Mainly aiming at characteristics of child growth, the invention provides a 5% glucose child nutrient solution which can supplement energy, magnesium ions, and potassium ions for children and is easy to be absorbed. The formula of the 5% glucose child nutrient solution of the invention is that the following components are added into 100 mL of injection water: 5000 mg of glucose, 141 mg of potassium chloride, 189 mg of anhydrous potassium acetate, 21.4 mg of sodium dihydrogen phosphate, 30.5 mg of magnesium chloride heptahydrate, 15 mg of potassium phosphate, and 20 mg of sodium pyrosulfite. The particular preparation method comprises concentrated preparation, diluted preparation, filling and sterilization.
EP2296661A1 Sgc stimulators, sgc activators and combinations thereof for the treatment of hearing impairment The invention provides pharmacological compositions comprising a stimulator or activator of the soluble guanylate cyclase (sGC) either alone or in combination for the treatment of hearing impairment i.e. hearing loss and tinnitus.
CN1813848A Medicinal composition for treating osteo porosis and its formulation The present invention relates to a medicine composition for curing osteoporosis and its preparation. Said medicine composition is formed from (by wt%) 1%-15% of cnidium seed total coumarin, 1%-15% of epimedium total flavone, 1%-10% of drynaria root extract and 60%-97% of calcium citrate malate, and its preparation has two types of solid preparation and liquid preparation.
US20060134767 Mitotic kinesin binding site The present invention is directed to the identification, characterization and three-dimensional structure of a novel ligand binding site of KSP. Binding of ligands to the novel binding site result in a conformational change in the three-dimensional structure of the protein and a modulation of the activity of KSP. This conformational change in turn results in the formation of a novel binding pocket in the KSP protein, which comprises the novel binding site of the instant invention.
CN103275070A Tetracyclic compound for adjusting proliferation of mononuclear cells and application of tetracyclic compound The invention discloses a tetracyclic compound for adjusting the proliferation of mononuclear cells and an application of the tetracyclic compound. The tetracyclic compound is BJ-20201, and the name of the tetracyclic compound is (2R, 5S)-5-((S)-2-(benzofuran-2-carboxamido)-4-methylpentanamido)-N-(2-fluorobenzyl)-2-methyl-6-oxoazepane-1-carboxamide. The molecular structural formula of the tetracyclic compound is shown in the specification. The tetracyclic compound can be used for promoting the proliferation of mononuclear cells and treating cells of neurodegenerative diseases such as senile dementia, lateral sclerosis spinal cord and parkinsonian disease.
US20080194653 Using a thiadiazole drug; anticancer agents A therapeutic and/or prophylactic agent for a solid tumor, which comprises a thiadiazoline derivative represented by the general formula (I), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R1 represents a hydrogen atom, R2 represents lower alkyl, or R1 and R2 are combined together to represent alkylene, R3 represents lower alkyl, R4 represents NHSO2R6 (wherein R6 represents hydroxy or the like) or the like, and R5 represents aryl or the like] and the like are provided.
US20120322837 Amide compound and medicinal use thereof A compound of formula [I-W]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.
WO2014084494A1 Novel disubstituted adamantyl derivative or pharmaceutically acceptable salt thereof, production method for same, and pharmaceutical composition for suppressing cancer metastasis comprising same as active ingredient The present invention relates to a novel disubstituted adamantyl derivative or a pharmaceutically acceptable salt thereof, to a production method for same, and to a pharmaceutical composition for suppressing cancer metastasis or combating cancer comprising same as an active ingredient. The disubstituted adamantyl derivative according to the present invention suppresses the HIF-1 enzyme, which is associated with cancer metastasis, and so effects dose-dependent inhibition of the production of TWIST proteins, which are proteins associated with cancer metastasis, and thereby suppresses the consequent activities of beta-catenin and Rho proteins (RhoA), which are proteins associated with subsequent cancer metastasis, and of MMP2 and MMP9 which are genes associated with EMT, and as a result the derivative has an outstanding effect in inhibiting cancer cell metastasis and, in addition, the derivative is not cytotoxic and so has no cytotoxic side effects even when absorbed into the human body, and can therefore advantageously be used as a pharmaceutical composition for suppressing cancer metastasis or combating cancer.
CN101632640B Meloxicam liposome and pharmaceutical composition thereof The present invention provides a meloxicam liposome and a pharmaceutical composition thereof. The meloxicam liposome consists of one part by weight of meloxicam, 1.5-10 parts by weight of phospholipid, 1-3 parts by weight of cholesterin and 1-4 parts by weight of poloxamer 188. The invention is made in a such way that the meloxicam is made into the liposome, and the liposome is made into solid pharmaceutical preparation. The preparation components and the preparation art are simple, compared with the prior meloxicam preparation, the invention can not only improve the stability of the meloxicam solid preparation, but also can improve the dissolvability and the bioavailability of the meloxicam.
US20090192213 Benzo[b]furane And Benzo[b]thiophene Derivatives The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.
CN103463007A Application of racemosins A in preparation of medicine treating rhinitis Racemosins A treating immune inflammation is used for preparing the medicine treating the immune inflammation and is especially suitable for preparing the medicine treating the rhinitis. Compared with terfenadine and diclofenac sodium, the racemosins A is good in therapeutic effect. The application of the racemosins A in preparation of the medicine treating the rhinitis is disclosed for the first time. The matrix type of the racemosins A belongs to a brand new matrix type. The racemosins A has the advantages of being high in activity for treating the rhinitis and prominent in substantive features, and makes remarkable progress in preventing and treating the rhinitis.
US8105830 Polyspecific binding molecules and uses thereof The present invention relates to polyspecific binding molecules and particularly single-chain polyspecific binding molecules that include at least one single-chain T-cell receptor (sc-TCR) covalently linked through a peptide linker sequence to at least one single-chain antibody (sc-Ab). Further disclosed are methods and compositions for testing and using the molecules.
US20120029084 Topical Nepafenac Formulations Topical suspension compositions of nepafenac are disclosed. The compositions are especially suitable for topical ophthalmic administration.
CN101507787A Dietetic medicine preparation capable of promoting lactation and preparation method thereof The invention discloses a food and medicament dual-purpose preparation for stimulating lactation of lying-in women and a preparation method thereof. The food and medicament dual-purpose preparation is prepared from Chinese yam, Astragalus membranaceus, E-gelatin, liquorice dry extract powder, bean flour and vitamin E according to certain proportion. The food and medicament dual-purpose preparation for stimulating the lactation of the lying-in women has the efficacies of invigorating vital energy and enriching the blood, and relaxing vein and promoting the lactation, is convenient to take, has safe and reliable effect, is suitable for treating qi and blood deficiency and latex stasis caused by blood loss and qi consumption, qi and blood deficiency or weakness of the spleen and the stomach and insufficient, and qi and blood circulation in the intrapartum period, and overcomes the defects in the prior art.
US20080175794 Substituted Pyridazinyl- and Pyrimidinyl-Quinolin-4-Ylamine Analogues Substituted pyridazinyl- and pyrimidinyl-quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
US8153791 substituted pyrimidine compoundssuch as 4-amino-6-(3-chloro-4-fluoro-phenylamino)-pyrimidine-5-carbaldehyde O-methyl oxime, used for treating, preventing or ameliorating a chronic or acute protein kinase mediated diseasea, disorders or conditions The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.
CN102040601A 1-N-(1-azabicyalo(2,2,2) octane ether compound and application thereof The invention relates to a 1-N-(1-azabicyalo(2,2,2) octane ether compound and application thereof. The compound comprises a 1-N-(1-azabicyalo(2,2,2) octane ether compound, a mixture of optical isomers, diastereoisomers and enantiomers of the quaternary ammonium salt of the 1-N-(1-azabicyalo(2,2,2) octane ether compound, pharmaceutically acceptable salt compounds and pharmaceutically acceptable medical compositions of the 1-N-(1-azabicyalo(2,2,2) octane ether compound. The compound provided by the invention can be used for treating diseases or symptoms related to the cholinergic systems of the central nervous system (CNS) and the peripheral nervous system (PNS), symptoms related to neurodegeneration, diseases or symptoms of the gastrointestinal tract, the respiratory tract, and the like related to smooth muscle contraction, endocrine diseases or symptoms, diseases or symptoms related to inflammations, abstinence symptoms caused by withdrawals of drug abuse as well as ocular diseases, anesthesia, septic shocks, biliary colic, urogenital tract renal colic, bladder irritation diseases, and the like.
EP1838172A1 Novel nutraceutical compositions The present invention describes a composition which comprises one amino acid and a protein hydrolysate.
US20120190698 Methods of predicting thiopurine response The present invention relates to methods of predicting therapeutic efficacy of thiopurines in an individual by determining the presence of one or more risk variants. In one embodiment, the effective therapeutic efficacy of thiopurines is determined by the presence of risk variants at the genetic loci of HLA-DRB1, CREM, TAGAP, PLCL1, GPX4, SBNO2, MEF2A and/or LYSMD4. In another embodiment, the risk variants are located at the genetic loci of ARL4C, IL1R2, JAK2, 19q13, CARD9, SNAPC4, and/or 8q24. In another embodiment, the individual is has been diagnosed with inflammatory bowel disease.
CN1785168A Application of rugose soft sulfo-acid in anti HIV-1 virus An application of the multiplicate soft sulfonic acid in suppress the activity of HIV-1 virus is disclosed. Its advantages are high effect to HIV-I virus and low poison to host cell.
WO2012145374A1 TARGETING miR-378 FAMILY MEMBERS FOR THE TREATMENT OF METABOLIC DISORDERS Provided herein are methods and compositions for the treatment of metabolic disorders. Also provided herein are methods and compositions for improving insulin resistance, reducing blood glucose levels, and/or reducing blood insulin levels in a subject in need thereof. In certain embodiments, the methods comprise inhibiting the activity of one or more miR-378 family members. In certain embodiments, such methods comprise administering a compound comprising a modified oligonucleotide targeted to one or more miR-378 family members.
CN103356517A Application of Scopariusins in preparation of antibacterial medicines The invention relates to an application of Scopariusins in preparation of antibacterial medicines, and belongs to the field of medicines. The Scopariusins has strong functions of restraining escherichia coli, pseudomonas fluorescens, staphylococcus aureus, proteusbacillus vulgaris and cryptococcus neoformans, and therefore the Scopariusins can be used as a compound with an antibacterial function, and is expected to be applied to the preparation of related medicines. The application of the Scopariusins in the preparation of the antibacterial medicines is firstly disclosed. The framework type is a brand-new framework type, and therefore the Scopariusins is impossibly revealed by other compounds. The Scopariusins has outstanding substantive characteristics. Meanwhile, the Scopariusins has significant progress in preventing and treating bacterial infection.
US20080038195 radiolabeling; neurodegenerative diseases This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
WO2014143629A1 Bimatoprost for enhancement of leptin production Prostamides such as bimatoprost and its pro-drugs for enhancement of leptin production and appetite suppression.
EP2137146B1 Crystalline forms of atorvastatin 4-(nitrooxy) butyl ester The present invention relates to two crystalline forms designated as form A and form B, of (βR, δR) -2 (4-fluorophenyl) - β, δ-dihydroxy-5- (1-methylethyl) -3-phenyl-4- [ (phenylamino) carbon-yl] -1H-pyrrole-1-heptanoic acid 4- (nitrooxy) butyl ester (atorvastatin 4- (nitrooxy) butyl ester), represented by the formula (I), The invention also relates to processes for the preparation of the forms A and B, to pharmaceutical compositions comprising the two forms, and to their use for treating and/or preventing acute coronary syndromes, stroke, neurodegenerative disorders, such as Alzheimer's and Parkinson's disease as well as autoimmune diseases, such as multiple sclerosis.
US20100047195 Lip balm and method of treating lip conditions A pharmaceutical composition for treating a lip condition. The pharmaceutical composition includes a therapeutically effective amount of a corticosteroid, or a physiologically acceptable salt of the corticosteroid, and a physiologically acceptable carrier In the composition, the corticosteroid does not include hydrocortisone. Also provided is a method of using the composition to treat a lip condition such as inflammation or infection.
CN1872328A Application of medication composition of containing giant typhonium tuber in preparing medicine for treating insufficiency of blood supply for brain An application of the medicinal composition composed of 11 Chinese-medicinal materials including Chuan-xiong rhizome, red sage root, gastrodia tuber, borneol, etc in preparing the medicines for treating chronic cerebral ischemia is disclosed.
USRE39634 treatment of neuropathic pain; elevate levels of anandamide or other endogenous cannabinoids to increase the nociceptive threshold The present invention relates to bisarylimidazolyl derivatives and pharmaceutical compositions comprising said compounds inhibiting fatty acid amide hydrolase and useful for the treatment of pain, particularly neuropathic pain, psychomotor disorder, hypertension, cardiovascular disease, eating disorder, nausea, AIDS-related complex, glaucoma, inflammation, psoriasis or multiple sclerosis, and other conditions the treatment of which can be effected by inhibiting fatty acid amide hydrolase.
EP2461812A1 Composition for the treatment of cystic fibrosis The present invention provides compositions comprising a prostacyclin or prostacyclin analogue, or a pharmaceutically acceptable salt thereof for use in preventing or treating cystic fibrosis. The invention also provides the use of a kit comprising a prostacyclin or prostacyclin analogue for treating or preventing a condition associated with cystic fibrosis in a subject.
CN101475555B 1',2',3',7'-tetrahydrotheaflavine-3-digallate, and preparation and use thereof The invention provides a novel compound, which is 1',2',3',7'- tetrahydro theaflavin-3- digallic acid ester and the chemical structural formula thereof is shown as (2). The compound of the invention can be obtained by hydrogenating and reducing theaflavin-3- digallic acid ester, has the functions of inhibiting the activity of reverse transcriptase and the activity of HIV gp41 forming a six-strandhelical core structure, can prevent HIV virus from entering a host cell, and has stronger inhibiting functions on the activity of the reverse transcriptase and the activity of HIV gp41 forming the six-strand helical core structure than the theaflavin-3- digallic acid ester.
WO2013013490A1 Use of medicament targeting cyslt1 in preparation of drug for prevention or treatment of autoimmune diseases Provided is a use of a medicament targeting a cysteine-leukotriene receptor CysLT1 in preparation of a drug for prevention or treatment of autoimmune diseases. The antagonists of CysLT1 include Montelukast, Zafirlukast and Pranlukast, and are used for treatment or prevention of multiple sclerosis, rheumatoid arthritis, lupus erythematosus or inflammatory bowel disease.
CN103271918A Application of Myriberine A in preparing drug for treating endometrial cancer The invention discloses an application of Myriberine A in preparing a drug for treating endometrial cancer, and belongs to the technical field of novel drug applications. In-vitro MTT antineoplastic activity evaluation shows that Myriberine A has a significant inhibitory effect for the growth of human endometrial cancer cell line ISK and RL95-2. Therefore, Myriberine A can be used for preparing the drug for treating the endometrial cancer and has good development and application prospects. The application of Myriberine A in preparing the drug for treating the endometrial cancer is disclosed for the first time. Besides, the Myriberine A has an extraordinary inhibitory activity for endometrial cancer cells.
EP1572191A1 Pharmaceutical composition containing brevifoliol for use in chemotherapeutic treatment of human beings The present invention relates to the bioactivity of taxanes isolated from the leaves of Himalayan Yew tree Taxus wallichiana against human cancer cell lines grown in-vitro and subsequent identification of brevifoliol (1) as anticancer agent useful in the treatment of various types of cancer in humans.
US20100081723 Memantine For The Treatment Of Childhood Behavioral Disorders The present invention provides a method for the treatment of individuals diagnosed with a childhood behavioral disorder such as autistic spectrum disorders or combined type Attention-Deficit/Hyperactivity Disorder (ADHD) by administering an effective amount of memantine.
EP2407471A2 Process for preparing a crystalline form of rapamycin analogs A process for preparing a crystalline form of a rapamycin analog, which process comprises: combining the rapamycin analog with at least one organic medium to form a mixture that is saturated with the rapamycin analog; incubating the saturated mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog from the organic medium.
CN1943651A A medicinal composition for treating gout This is a medical composition for treating gout composed with analgin, ketoprofen, dry extract of stauntonvine, acetate prednisone, naproxen, vitamin B 6 and sodium bicarbonate. The medical composition is reasonable designed with obvious curative effect and fast effectiveness in treat gout. It is easy to take in with no rebound after stopping the medicine. There are complementary actions between the said medical ingredients with no harmfulness. The composition is a common medicine that can be used for long time but with low costs. It is safe, and its quality can be controlled.
CN101012227A Novel 13-n-octylberberine derivative with antineoplastic action The invention discloses a new synthesizing method of 13-n-octyl berberine (1) and 13-n-octyl palmatine (2) as berberine derivant and medical acceptable salt and liposome, which is characterized by the following: inhibiting the growth of cancer cell obviously through S180 transplanted tumour model test under lower dose condition; saving cost.
CN102114187B Ointment for nourishing and promoting tissue regeneration and production method thereof The invention relates to an ointment for nourishing and promoting tissue regeneration and a production method thereof. An ointment product for nourishing and promoting the tissue regeneration is prepared from the following pharmaceutical materials in parts by mass: 17-20 parts of scutellaria baicalensis root, 17-20 parts of phellodendron, 17-20 parts of liquorice root, 17-20 parts of common bletilla tuber, 17-20 parts of sinkiang arnebia root, 1-1.5 parts of borneol, 6-6.5 parts of borax, 17-20 parts of ligusticum chuanxiong hort and 6-6.5 parts of gecko powder. The production method comprises the steps of washing the scutellaria baicalensis root, the phellodendron, the liquorice root, the common bletilla tuber, the ligusticum chuanxiong hort and the gecko powder, drying for four hours ata temperature of 105 DEG C, smashing together with the sinkiang arnebia root, passing through a sieve with 120 meshes, adding the borneol and the borax, uniformly grinding, adding a cream matrix and uniformly grinding to obtain the ointment for nourishing and promoting tissue regeneration. The ointment is used for dressing change of trauma and infected wound, and has strong effects of resisting bacteria, diminishing inflammation, promoting the tissue regeneration, activating blood circulation and the like and the advantages of definite efficacy and no adverse reaction. Moreover, due to simplicity in preparation method and low requirements on equipment, the ointment is suitable for small and medium-sized medicine production enterprises or a preparation room of a medical institute for mass production.
US20120329875 Ibuprofen for Topical Administration Set forth herein is a preparation of ibuprofen (2-(4-isobutylphenyl) propionic acid) in the free acid form that is suitable for topical administration. The topical ibuprofen formulation is prepared by dissolving the free acid form of ibuprofen, or preparing a homogeneous suspension of the free acid form of ibuprofen, in the presence of a pharmaceutically acceptable solvent so as to produce a topical drug formulation compatible with the penetration of 2-(4-isobutylphenyl) propionic acid through the skin tissue. Topical formulations of ibuprofen can be based on a pharmaceutically acceptable solvent such as, e.g., a pyrrolidone solvent or dimethylacetamide.
CN102872142A Application of Houttuynoid D in drug for treating ovarian cancer The invention discloses application of Houttuynoid D in preparing a drug for treating human ovarian cancer, belonging to the technical field of the new use of the drug. Houttuynoid D is found to have obvious inhibition effect on the growth of human ovarian cancer cell lines HO-8910, HOC1 and OVAC through MTT (Methyl Thiazolyl Ternzolinm) anticancer activity evaluation in vitro. Therefore, Houttuynoid D can be used for preparing the anti-ovarian cancer drug and has excellent prospects in development and application. The use of Houttuynoid D in preparing the drug for treating the human ovarian cancer involved in the invention is disclosed for the first time; the framework type of Houttuynoid D is a brand new framework type; and Houttuynoid D has an unexpectedly high inhibition activity for the human ovarian cancer cells.
CN101357122A Use of carbon monoxide released substance in preparing medicine for treating pyemia The invention discloses the application of carbon monoxide derived substance in preparing the medicine which cures sepsis. In the invention, methylene dichloride is dissolved in edible benne oil and prepared to the formulation which is used for oral; after the formulation is taken orally and absorbed, the formulation can unceasingly release carbon monoxide in body, therefore, the formulation can be used as an extrinsic carbon monoxide donator, and is intervened and tested by a mouse CLP sepsis model, the result is that the oral formulation can serve as a medicine which inhibits sepsis in early stage. The sepsis is inhibited by the oral formulation, the concentration of can be relatively easily controlled; when the oral formulation is used for long term, superadditon is convenient; therefore, the formulation can meet the requirements of clinical application.
US20090253674 Substituted Triazole Derivatives As Oxytocin Antagonists The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
US20070009444 Method for preparing powder exhibiting low susceptibility to electrification A method of producing lowly-charged powder comprising drying a liquid composition containing a highly-charged compound and polyethyleneglycol.
US20120213768 Diagnostic and Therapeutic Uses for B Cell Maturation Antigen Biomarkers and therapies against autoimmune diseases, including systemic lupus erythematosus (SLE) are described herein. The present invention is based on the discovery of B cell maturation antigen (BCMA) and BCMA variant expression on SLE monocytes that can be directly associated with disease activity. The findings of the present invention enable the design of monoclonal antibodies or recombinant proteins that can block BCMA and BCMA variants as well as BCMA-bound APRIL.
CN103565783A Application of hexachlorophene in preparation of voltage-gated potassium channel agonist The invention provides an application of hexachlorophene in the preparation of a KCNQ agonist. In addition, the invention provides an application of the hexachlorophene in the preparation of a medicine serving as the KCNQ agonist. In the application, the KCNQ agonist can be a KCNQ1 agonist, a KCNQ1/KCNE1 agonist, a KCNQ2 agonist or KCNQ2/KCNQ3 agonist. The hexachlorophene has the effects of shortening the action potential duration and treating the arrhythmia by boosting KCNQ1/KCNE1 electric currents and promoting the repolarization of the action potential of myocardial cells. The subtype potentiation proves that the hexachlorophene is capable of enhancing KCNQ and M electric currents and has the effects of adjusting the membrane potential level by boosting KCNQ2 electric currents and KCNQ2/KCNQ3 hetero-oligomer electric currents and weakening the issuing frequency of the action potential; the application of the hexachlorophene in the preparation of medicines taking KCNQ as anti-epileptic targets is realized, and the anti-epileptic effect is achieved.
EP2066673A2 Tricyclic compounds and its use as tyrosine kinase modulators Provided are compounds of formula (I) or a stereoisomer, tautomer, salt, hydrate or prodrug thereof, capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use.
US20120171283 Liposomes Useful for Drug Delivery The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provides methods of making the liposome compositions provided by the present invention.
CN103239464A Application of icarisid II in preparation of sensitizer for chemotherapic medicine The invention belongs to the field of biological medicines, and relates to application of icarisid II in preparation of a sensitizer for a chemotherapic medicine. Shown in the experimental results, the icarisid II can obviously improve the inhibition effect of the taxol to the cancer cell proliferation, the taxol-induced tumor cell apoptosis, and the effect of inhibiting a TLR4 (Toll-Like Receptors 4) patch in order to improve the sensitivity of a chemotherapeutic medicine; the icarisid II can be used as the sensitizer for the chemotherapic medicine, and is applied to the tumor chemotherapy process, in order to obviously promote the medicine sensitivity of different tumor cells to the chemotherapic medicine, therefore, the dosage of the chemotherapic medicines is decreased, and the toxic and side effects of the chemotherapic medicine to normal cells of a human body are reduced. The icarisid II can be used as an active ingredient to be used together with a pharmaceutically acceptable carrier in order to prepare a pharmaceutical composition performing sensibilization in tumor chemotherapy, and the pharmaceutical composition is applied to chemosensitization for a plurality of tumors, including but not limited to melanoma and cutaneous squamous cell carcinoma and the like.
WO2007034757A1 Remedy for amyloid diseases and drug for monitoring the same A styrylbenzene derivative represented by the following chemical formula (1) has an effect of inhibiting the coagulation or fibrosis of an amyloid protein: wherein R1 and R2 independently represent hydroxyl or carboxyl; and R3 represents fluorine or bromine. Because of being capable of inhibiting a structural change in an amyloid protein accompanying an amyloid disease, the above-described styrylbenzene derivative is efficacious in treating amyloid diseases. In addition, it has an affinity for an amyloid protein and, therefore, is effective in detecting amyloid proteins. Accordingly, use of the above compound enables both of the treatment and monitoring of amyloid diseases.
CN102793687A Cefaclor capsule and preparation method thereof The present invention relates to a cefaclor capsule and a preparation method thereof. The cefaclor capsule is composed by the following components by weight: 100 parts of cefaclor, 5-100 parts of pregelatinized starch, 1-5 parts of silica and 0.5-2.5 parts of magnesium stearate. The preparation method comprises: (1) sieving the cefaclor after pulverization; (2) mixing pregelatinized starch and silica with the sieved cefaclor powder uniformly; (3) adding magnesium stearate and mixing uniformly; and (4) making the mixed powder into capsules, and packing the qualified capsules into resulting products after detection. The sources of raw and auxiliary materials selected by the present invention are convenient. The auxiliary materials are few in types, are all commonly used auxiliary materials for preparations, and are low in prices. The production process is simple, and the operation is convenient and fast. The preparation process is simple, easy in operation, low in cost, and high in yield, and is suitable for large-scale industrial production.
CN103202838A Plant extract composition with liver protecting effect The invention relates to a plant extract composition with a liver protecting effect. The composition contains sulforaphane, silymarin, curcumin and the like. The sulforaphane is an extract of a cruciferous plant such as cauliflower seeds and broccoli, the silymarin is an extract of a compositae medicinal plant such as silybum marianum, and the curcumin is an extract of a plant such as turmeric. The composition consisting of the sulforaphane, the silymarin and the curcumin in a weight ratio of 1: (10-50): (10-50) is a novel health product with the liver protecting effect.
US20100254962 Functional drink The invention relates to a liquid food product as aqueous solution with anti-ageing effect, which comprises resveratrole, citric acid, fructose, black grape polyphenol extract, green tea extract, vitamin E, vitamin C and niacin. A concentrated juice from red, edible soft fruit is present at least in a sufficient amount to impart the taste, and advantageously the colour, of the formulation.
US20080166293 Receptor-mediated uptake of peptides that bind the human transferrin receptor Peptides have been discovered which are capable of binding to and internalizing with the human transferrin receptor (hTfR). The sequences HAIYPRH (Seq. ID No. 1) and THRPPMWSPVWP (Seq. ID No. 2) are capable of binding to and internalizing with the human transferrin receptor. When these molecules were fused with other molecules, the fusion product was internalized in cells expressing hTfR. The sequences have use for targeting other peptides and proteins into cells expressing hTfR.
US20110015200 Nitrogen-containing bycyclic compounds active on chronic pain conditions The invention refers to compounds of general formula (I) wherein the R groups are, independently, H, C1-6alkyl, aryl, CF3; Y is CH2, C═O; X is bond, C═O, SO2, or C═N—CN; m is 0, 1; n is 0, 1; A is a heterocycle, or a phenyl group optionally substituted as defined in the specification. The compounds are active on chronic pain conditions of different origin; they can be administered alone or with other drugs. Most of these compounds are new. The invention include a process to prepare said compounds, and pharmaceutical compositions suitable for their administration to a patient.
WO2006126654A1 Novel compound colletoic acid A novel compound having an inhibitory effect on 11β-hydroxysteroid dehydrogenase type 1 (hereinafter referred to as '11β-HSD1'); a pharmaceutical comprising the compound as an active ingredient (preferably a therapeutic/ameliorating agent for diabetes, obesity, hyperlipemia, hypertension or metabolic syndrome that develops these conditions compositery; a method for producing the compound; a novel microorganism capable of producing the compound; and others.
CN101342142B Temperature sensing in situ gel rubber formulations capable of being injected, preparation method and uses thereof The invention relates to injectable temperature sensitive in situ gel preparation and a preparation method as well as an application thereof. The components of the preparation of the invention comprise 0.01 percent to 10 percent of anticancer drugs, 15 percent to 25 percent of pluronic F127, 0.01 percent to 20 percent tween and 45 percent to 84.98 percent of water or buffer solution.
CN103251054A Anti-fatigue health protection food composition and preparation method thereof The invention relates to an anti-fatigue health protection food composition and a preparation method thereof. The anti-fatigue health protection food composition comprises the following materials in percentage by weight: 20-35 percent of a rhodiola extract, 10-20 percent of a guarana extract, 10-20 percent of an astragalus extract, 3-5 percent of vitamin C, 3-5 percent of vitamin E, 2-5 percent of nicotinic acid and the balance of edible auxiliary materials. On the basis of a fatigue generation mechanism and with combination of modern pharmacological research results, the rhodiola extract, the guarana extract and the astragalus extract are taken as the main raw materials for timely supplementing the consumption of internal energy substances, quickly resisting fatigue and recovering strength, reliving brain fatigue and improving the durability and the working efficiency in a fatigue state. By the reducing nutritious substances, such as the vitamin C and the vitamin E, the radical level and the oxidization stress reaction in vivo in the fatigue state are reduced and alleviated, the fatigue can be effectively alleviated, and the anti-fatigue health protection effect is enhanced.
WO2007133108A1 Pharmaceutical composition, method for the production and the use thereof The invention relates to a pharmaceutical composition comprising compounds which are used in the form of active substances and contain a 1-oxo-3-(1H-indol-3-il)-1,2,3,4-tetrahydroisoxynoline fragment, to a method for producing said compositions and the use thereof for treating and preventing the development of different diseases associated with an increased activation of the adrenocorticotropic hormone (ACTH) and to the use of compounds which contain the 1-oxo-3-(1H-indol-3-il)-1,2,3,4-tetrahydroisoxynoline fragment in the form of 'molecular pharmacological tools' for investigating (in vitro and in vivo) biochemical mechanisms of the action of corticosteroid hormones and of the specific receptors thereof, in particular, a melanocortin receptor-2 (MC2R) whose agonist is embodied in the form of a ACTH.
WO2013077579A1 Pharmaceutical composition for preventing and treating ophthalmic disorders The present invention relates to a composition for the prevention and treatment of ophthalmic disorders, characterized by containing a compound of formula (1) in the specification, and to a pharmaceutically acceptable salt or an isomer thereof. Furthermore, the present invention relates to a composition comprising the active ingredient for cleansing and preserving contact lenses.
US20080279812 Disease Prevention and Vaccination Prior to Thymic Reactivation The present disclosure provides methods for preventing or treating illness, improving responsiveness to immunization, and improving the efficacy of gene therapy in a patient by disrupting sex steroid signalling in the patient, wherein the bone marrow and other immune cell functionality is improved without, prior to, or concurrently with, thymic regeneration. In some embodiments, sex steroid signalling is interrupted or ablated in the patient by the administration of LHRH agonists, LHRH antagonists, anti-LHRH receptor antibodies, anti-LHRH vaccines, anti-androgens, anti-estrogens, selective estrogen receptor modulators (SERMs), selective androgen receptor modulators (SARMs), selective progesterone response modulators (SPRMs), ERDs, aromatase inhibitors, or various combinations thereof.
CN1879628A An in-vitro trichomonas vaginalis treating vaginal suppository and preparation method thereof The invention relates to a suppository for treating vaginal trichomonas in vitro and its preparation, wherein the main compositions of the suppository include metronidazole 0.8-1.2 parts, dihydro-artemisinin 1.6-2.4 parts, cocoa bean grease 40-60 parts.
CN101235059B Phenylpropanoids derivatives, preparation method thereof and medical composition using the same as active component The invention relates to a phenylpropanoids derivative of formula (I), wherein R represents hydrogen. The invention further relates to a corresponding preparation method, a drug composite which uses the compound as active component and an application of the compound and the drug composite in the treatment of breast cancer, nasopharyngeal carcinoma, cervical cancer, HepG-2 liver cancer and A549 lung cancer.
US20090105248 3-monosubstituted tropane derivatives as nociceptin receptor ligands Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—(CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.
CN101357158A External medicine for treating summer diarrhea and preparation method thereof The invention provides an external medicine used for treating summer diarrhea, which is made of the following bulk drugs by weight percentages: 10-18% of flavescent sophora root, 10-18% of licorice and 64-80% of talc; the bulk drugs are taken out in proportion and crushed to be 40-500 mesh fine powder, then the powder is evenly mixed and filled in cloth bags. The medicine has the efficacies of clearing away pathogenic heat, eliminating dampness and removing the toxin, can cause the heat and the dampness to be respectively eliminated, thus stopping the diarrhea. The medicine has good effect on bellyache and the diarrhea complicated by pyrexia, thirst and scanty dark urine caused by the summer diarrhea.
CA2150229C Nitric esters having a pharmacological activity and process for their preparation Nitric esters with pharmacological activity having general formula (I), their pharmaceutical utilisation and process for their preparation.
US20110201581 Novel Compounds 010 The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
WO2006131807A1 Preparation of 3-amino-4,5-disubstituted-pyrazole derivatives A process for preparing a compound of Formula (I) is described herein as well as rocesses for using this compound to prepare other useful intermediates and compounds.
CN102743563A Anticancer beverage The invention provides a anticancer beverage, comprising the components of, by weight, 200-300 parts of ginseng, 50-100 parts of garlic, 10-20 parts of cortex magnoliae officinalis, 5-10 parts of majoram, 20-35 parts of folium artemisiae argyi, 5-10 parts of perilla, 10-20 parts of whole ginseng, 10-20 parts of rutin, 5-10 parts of cinnabar, 5-10 parts of lignum dalbergiae odoriferae and 5-20 parts of arsenolite. The anticancer beverage can improve internal body immune system via an internal modulation method to reach an object of anticancer, and is simple in operation and convenient to drink.
WO2013141264A1 Novel cysteine compound and salt thereof The purpose of the present invention is to provide a novel compound with Eg5 inhibiting activity that is useful as an antitumoral agent. The present invention pertains to a compound expressed by the general formula (I) (in formula (I), A represents Ch2, a sulfur atom, or an oxygen atom; and R represents a halogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group, or a trifluoromethyl group) or a salt thereof.
EP1551810B1 Diaryl-substituted cyclic urea derivatives having an mch-modulatory effect The invention relates to substituted diaryl heterocycles and the physiologically compatible salts and physiologically functional derivatives thereof. The invention also relates to compounds of formula (I) wherein the radicals have the cited designations, to the physiologically compatible salts thereof, and to methods for producing the same. Said compounds are suitable, for example, as anorexiants.
CA2210998C Inhibition of neovascularization using vegf-specific oligonucleotides Disclosed are methods of reducing neovascularization and of treating various disorders associated with neovascularization. These methods include administering to a tissue or subject a synthetic oligonucleotide specific for vascular endothelial growth factor nucleic acid effective in inhibiting the expression of vascular endothelial growth factor.
US6979687 Theophylline-based soluble guanylyl cyclase activators KMUP-1 analogues enhanced cyclic GMP and K+ channel activities on rabbit corpus cavernosum smooth muscle and intercavernous pressure activities The invention pertains to theophylline (1-methyl, 3-methyl xanthine) and IBMX (1-methyl, 3-isobutyl xanthine) derivatives of formulas I and II: where R1 is —CH3 or —CH2CH(CH3)2, and R2 is where R3 and R4 are independently selected from the group consisting of OCH3, CH3, NO2, F, Cl, Br and I.
WO2013021038A1 Bicyclic labdane diterpenes for use in the treatment of trpc6 associated diseases The present invention relates to bicyclic labdane diterpenes for use in the treatment of a disease associated with activation of transient receptor potential cation channel 6 (TRPC6), preferably a pulmonary or a renal disease. In one aspect the invention relates to the use of a bicyclic labdane diterpene for blocking calcium transport via TRPC6. Another aspect of the invention is a bicyclic labdane diterpene according to formula (1) for use as a medicament wherein R1 is selected from hydrogen and C1 to C4 acyl, wherein the bicyclic labdane diterpene optionally comprises at least one double bond between the carbon atoms at positions 1 and 2, 2 and 3, 5 and 6, 6 and 7 and/or 14 and 15, wherein the carbon atoms at positions 1, 2, 3, 7, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20 are connected to hydrogen atoms or comprise at least one substitution.
WO2005118559A1 A type of formyl peptide receptor-like 1 regulator, preparation method and use thereof The present invention relates to a type of novel formyl peptide receptor-like 1 regulators which have the following structure, and their uses in preparing the medicines of antünflammation, antünfection and immunoregulation. The present invention also relates to the preparation method of these compounds.
WO2007017695A3 Dihydroxyanthraquinones and their use A compound of formula (1), wherein X is H or -OC R1 and Y is H or -OCR2, provided that X and Y are not both H; and R is CH2OR9, CONR11R12, CN, tetrazole or COOR17; or a salt thereof, has therapeutic utility.
US20090131428 Benzooxazole-4,7-dione, derivatives and their use as cdc25 phosphate inhibitors The invention concerns the use as cdc25 phosphatase inhibitors, in particular cdc25-C phosphatase, and CD45 phosphatase, of compounds of general formula (I), wherein: W represents O or S. In accordance with the invention, the compounds of general formula (I) can in particular be used for preparing a medicine for cancer treatment.
CN101531691A Triazole glucoside, method for synthesizing same by enzyme chemical method and application thereof The invention relates to triazole glucoside, a method for synthesizing the same and application thereof. The triazole glucoside is synthesized by a two step system and a one kettle way according to the following steps: saccharide and alcohol containing alkynyl or azido perform a glycosylation reaction under glycosidase catalysis to generate a glucoside compound containing terminal alkynyl or nitrine; and the glucoside compound containing terminal alkynyl or nitrine and organic nitrine or alkyne generate the target product, namely the triazole glucoside by addition cyclization under cuprous catalysis. The triazole glucoside can be used for preparing medicament, in particular antifungal medicament.
US8697055 Probiotic, lactic acid-producing bacteria The present invention discloses compositions and methodologies for the utilization of probiotic organisms in therapeutic compositions. More specifically, the present invention relates to the utilization of one or more species or strains of lactic acid-producing bacteria, preferably strains of Bacillus coagulans, for the control of gastrointestinal tract pathogens, including antibiotic-resistant gastrointestinal tract pathogens, and their associated diseases by both a reduction in the rate of colonization and the severity of the deleterious physiological effects of the colonization of the antibiotic-resistant pathogen.
CN102875464A 3-Schiff base-2(1H)-quinolinone derivative and preparation method and application thereof The invention discloses a 3-Schiff base-2(1H)-quinolinone derivative and a preparation method and application thereof. The 3-Schiff base-2(1H)-quinolinone derivative is prepared by disposing 3-formaldehyde base-2(1H)-quinolinone or 3-formaldehyde base-6 methyl-2(1H)-quinolinone, primary-amine-contained compound and organic solvent into a reactor and condensing at the temperature of 80-100 DEG C. Compared with antioxidant activity of the 3-formaldehyde base-2(1H)-quinolinone or the 3-formaldehyde base-6 methyl-2(1H)-quinolinone, the antioxidant activity of the 3-Schiff base-2(1H)-quinolinone derivative is enhanced obviously. The structural formula thereof is shown as the formula (I), wherein the R1 is H or methyl, and the R2 is aromatics substituent or aliphatic hydrocarbon substituent.
CN101928320B American ginseng ginsenoside F5ab and extraction method and medicinal application thereof The invention relates to American Ginseng ginsenoside F5ab and extraction method and medicinal application thereof, and belongs to a novel compound and the medicinal application thereof. The American ginseng as a raw material, is subjected to water extraction, adsorption of macroporous adsorbent resin, silica column chromatography, and recrystalization to form a novel compound which has the chemical name of 3-O-beta-D-glucopyranosyl-(1-2)-beta-D-glucopyranosyl-20-O-beta-D-xylopyranosyl-dammar-25(26)-ene-3beta,12beta,20S,24zeta-tetraol, which is called as American Ginseng ginsenoside F5ab for short. The yield is over 0.01 percent. The American Ginseng ginsenoside F5ab has wide medicinal application to preparing medicaments for treating myocardial ischemia.
US20060122271 Stable gabapentin having pH within a controlled range A pharmaceutical composition containing substantially pure and stable gabapentin are disclosed wherein gabapentin has a pH of between 6.8 to 7.3.
US20100137405 RNA Interference Mediated Inhibition of Cyclic Nucleotide Type 4 Phosphodiesterase (PDE4B) Gene Expression Using Short Interfering Nucleic Acid (siNA) The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression and/or activity, including PDE4B1, PDE4B2, and PDE4B3 gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions, including but not limited to IL-6, IL-I, IL-8, IL-15, TNF-alpha and matrix metalloproteinases (MMPs), such as MMP-I, MMP-2, MMP-3, MMP-9 and MMP-12. Specifically, the invention relates to double stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA), and multifunctional siNA molecules capable of mediating RNA interference (RNAi) against cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression, including cocktails of such small nucleic acid molecules and lipid nanoparticle (LNP) formulations of such small nucleic acid molecules. The present invention also relates to small nucleic acid molecules, such as siNA, siRNA, antisense and others that can inhibit the function of endogenous RNA molecules or RNAi pathway components (RNAi inhibitors), such as endogenous micro-RNA (miRNA) (e.g, miRNA inhibitors) or endogenous short interfering RNA (siRNA), (e.g., siRNA inhibitors) or that can inhibit the function of RISC (e.g., RISC inhibitors), to modulate PDE4B gene expression by interfering with the regulatory function of such endogenous RNAs or proteins associated with such endogenous RNAs (e.g., RISC) including cocktails of such small nucleic acid molecules and lipid nanoparticle (LNP) formulations of such small nucleic acid molecules. Such small nucleic acid molecules are useful, for example, in providing compositions to prevent, inhibit, or reduce inflammatory, respiratory, and autoimmune diseases, traits, and conditions, and/or other disease states associated with PDE4B gene expression or activity in a subject or organism.
EP1198239B1 METHODS EMPLOYING BACTERIAL ParD kis/ParD kid TOXIN-ANTITOXIN SYSTEM FOR KILLING EUKARYOTIC CELLS A method of inhibiting cell proliferation and/or cell cycle progression, the method comprising providing within eukaryotic cells a bacterial toxin, in particular a bacterial toxin of a post-segregational killing system such as ParD. Activity or production of toxin and/or inhibitor, e.g. antidote, are controlled for selective killing of target cells, not-target cells. Target cells include tumour cells.
CN101019897A Antitumor medicine composition and its prepn The present invention discloses one kind of antitumor medicine composition and its preparation process. The antitumor medicine composition consists of aweto and saponin. The present invention provides also the antitumor use of the medicine composition.
WO2006026829A1 Stable paste composition of enteric coated acid labile active agent and use thereof The present invention is concerned with an oral, non-aqueous, stable, ready-to-use, paste formulations containing an acid labile active component, such as a proton pump inhibitor, suitable for administration to mammals.
WO2005016323A3 Use of c-kit inhibitors for treating type ii diabetes The present invention relates to a method for treating type II diabetes, comprising administering a compound capable of depleting mast cells to a human in need of such treatment. Such compounds can be chosen from non-toxic, selective and potent c-kit inhibitors.
EP1782806A1 Compositions for treating dermatological and neurological disorders The present application relates to compositions and the treatment of skin disorders, dry skin, protection of skin in inflammatory events and neurological disorders. The present application more particularly discloses the identification of new genes and metabolic pathways involved in skin disorders, which provide novel targets and approaches for treating said disorders and for screening biologically active compounds. The present invention also provides various products and constructs, such as probes, primers, vectors, recombinant cells, which can be used to implement the above methods. The invention may be used to detect or treat various skin disorders, particularly dry and inflammatory skin disorders and neurological disorders, in various subjects, including mammalian subjects, particularly human beings.
US7863313 Methods for the treatment of inflammatory diseases Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for.
US20100035992 Methods and Compositions for Treating Inflammation and Inflammation-Related Pathologies Methods and compositions are provided for the treatment of inflammation and disorders, diseases, and adverse conditions, i.e., pathologies, caused by or otherwise associated with inflammatory processes. A metal ion sequestering agent that directly or indirectly exerts an anti-inflammatory effect is administered to a subject in combination with a sequestration inactivating moiety that facilitates transport of the metal ion sequestering agent through biological membranes. The sequestration inactivating moiety also inactivates the metal ion sequestering agent until association between the two components is cleaved in vivo to release the active sequestering agent. Compositions containing a metal ion sequestering agent and a sequestration inactivating moiety are also provided; the compositions optionally contain an added anti-inflammatory agent.
CN101744853A Antineoplastic drug taking panaxadiol saponins as active ingredient and application thereof The invention relates to the technical field of medicine, and provides an antineoplastic drug taking panaxadiol saponins as active ingredient and an application of panaxadiol saponins for preparing the antineoplastic drug. The invention discloses panaxadiol saponins with antineoplastic activity, both trypan blue dye exclusion method and MTT method indicate that panaxadiol saponins can inhibit the growing of tumor cells; and protein immunoblotting method indicates that panaxadiol saponins can lower the expression level of thioredoxin and cyclins D1 in tumor cell.
CN103724190A Compound EngyodontiuminA in secondary metabolites of deep sea fungi as well as preparation method and application thereof The invention discloses a compound EngyodontiuminA in secondary metabolites of deep sea fungi as well as a preparation method and an application thereof. The compound has a structural formula shown in the specification, a molecular formula of C12H15ClO4 and the molecular weight being 258.0659, is prepared by inoculating Engyodontium album mycelia in seawater, has an antibacterial function, and can be used for preparing antibacterial drugs.
CN101007006A Compound berberine sulphate injection and its preparation method The invention disclosed a kind of compound sulphuric acid berberine injection as well as its preparing method. The compound sulphuric acid berberine injection includes the following ingredients: 5-30 shares of suphuric acid berberine, 5-35 shares of mequindox, 1-25 shares of lactic acid trimethoprim and 0.5-2 shares of atrop; the preparing procedure includes the following steps: weighting ingredients; putting mequindox into the water for injection at 40-50DEG C; adding certain amount of auxiliary solvent, stirring for 10min to the solution is clear; putting lactic acid trimethoprim and atrop I to the previous solution, stirring and regulating the pH value; putting activated char into the solution and stirring for 15-20min, adding water for injection to 1000 shares to get the product. The invention can be widely used to treat the diarrhea caused by swine dysentery bacilli, increase its immunity and increase the body weights.
US20060135571 Imidazo(2,1-b)-1,3,4-thiadiazole sulfoxides and sulfones This invention relates to novel imidazo[2,1-b]-1,3,4-thiadiazole sulfoxide and sulfone compounds of Formula (I) and the use of compounds of Formula (I) in the treatment of neuronal disorders of the central and peripheral nervous systems and for the treatment of proliferative diseases such as cancer.
US20120071546 Novel Glutamic Acid Decarboxylase (GAD) Chimera And Methods Of Use The invention relates to a novel Glutamic Acid Decarboxylase (GAD). More specifically, novel DNA and protein sequences relating to GAD. Additionally, the invention discloses a novel composition and related methods for treating neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, epilepsy, and the like, using viral and non-viral delivery systems that deliver therapeutic agents to specific regions of the brain. More specifically, using an adeno-associated viral vector to deliver a nucleotide sequence encoding a novel glutamic acid decarboxylase (GAD) to specific regions of the brain that are over stimulated or disinhibited in various diseases, including neurodegenerative diseases
CN101747331B Isoniazid thiadiazine thione derivative The invention discloses an isoniazid thiadiazine thione derivative, which solves the problem that the existing derivative has poor lipid solubility of active ingredient, and can not dissolve in water or can not highly disperse. The structure of the derivative can be presented by INH-THTT-R-THTT-INH, wherein ING represents the structure of isoniazid of antitubercular drug, THTT is a ring structure, and R is linear chain, non-linear chain or annular alkyl compound containing two primary amines (including alkyl structures of different substituent groups). The derivative can be prepared into highly-dispersed drug delivery system, including the dosage form of liposome, solid lipid nanospheres, niosomes, micro emulsion and the like. The derivative can not only improve the lipid solubility of isoniazid, but also hydrolyze and release isoniazid active compound in vivo, increases the penetrability of isoniazid cell, reduces the tolerance of isoniazid during therapy and improves the curative effect.
CN101411686A Clarithromycin sub-microemulsion injection and preparation method thereof The invention belongs to the field of pharmaceutical preparation, and in particular relates to a clarithromycin submicron emulsion injection using phospholipid compound to carry medicine and a preparation method thereof. By 100 milliliters of the injection, the clarithromycin submicron emulsion injection comprises 0.05 to 0.5 gram of clarithromycin phospholipid compound in terms of clarithromycin, 10 to 20 grams of medium chain fatty acid triglyceride, 0 to 10 grams of soybean oil for injection, 0.2 to 2 grams of soya lecithin, 0.2 to 1 gram of Pluronic F-68, 0 to 0.5 gram of Tween-80, 0.01 to 0.05 gram of L-cysteine, 0.05 to 0.3 gram of sodium oleate, 2 to 5 grams of glycerin, and 70 to 90 grams of water for injection, wherein the mass ratio of clarithromycin in the clarithromycin phospholipid compound to the soya lecithin is between 1 to 1 and 1 to 12. The clarithromycin submicron emulsion injection has the advantages that the clarithromycin submicron emulsion injection has physical and chemical properties meeting requirement of medicine use for veins, not only can sterilize at high temperature, but also has favorable physical and chemical stability for long term storage, has little stimulation to the veins, improves adaptability of a patient, and is suitable for clinical application.
US20120295968 Pharmaceutical Composition Comprising Cannabinoids The present invention relates to a pharmaceutical composition comprising Δ9 Tetrahydrocannabinol (THC), Cannabidiol (CBD), and at least one small molecule selected from Citric Acid, Ascorbic Acid, Citrus Essential Oil(s), Lecithin, one or more sugar(s), Resvertrol, and combinations thereof, wherein the composition exhibits an increased but negated psychoactivity with concurrent enhancement in therapeutic potency of THC and/or CBD. The present invention is further directed to methods of treating one or more disease(s) or disorder(s) modulated by the activation of the Cannabinoid CB1 and/or CB2 receptors, by administering a therapeutically effective amount of the composition of the present invention to a subject in need thereof.
US7754205 Composition for transmucosal administration containing conenzyme Q as the active ingredient The present invention relates to the supply of coenzyme Q which is highly useful in maintaining human health, and provides a method and preparations whereby coenzyme Q can be efficiently supplied to patients having difficulties in oral administration, aged having swallowing difficulties and patients with diseases caused by topical disorders. It is found that the coenzyme Q concentration in the blood or topical mucosae can be elevated by using a composition for transmucosal administration containing oxidized coenzyme Q and/or reduced coenzyme Q as the active ingredient, wherein the total content of the oxidized coenzyme Q and the reduced coenzyme Q amounts to 0.0001 to 99% by weight of the whole composition.
US20110136916 6-shogaol for using in a method for the treatment of leukemia The present invention relates to the field of natural drugs, particularly to 6-shogaol for using in a method for the treatment of leukemia. The present invention provides a method for treating leukemia by applying a therapeutically effective dose of 6-shogaolt and this therapeutic method can be used for treating leukemia in mammals including human being.
CN103340872A Anti-depression use of evodiamine The invention relates to the drug field and in particular relates to an anti-depression use of evodiamine. According to the bodyweight appearance observed in a chronic unpredicted stress model test of the rat as well as the results of a sweet water preference test, an open-field test, a forced swinging test and the like, the evodiamine is proved to have an obvious improving effect. By virtue of the test of restraining the influences of the evodiamine to rat hippocampus monamine neurotransmitter and the influences to mouse behavior changes of reserpine-associated depression model, the anti-depression effect of the evodiamine is further proved.
US20110020325 Methods for reducing granulomatous inflammation This document provides methods and materials for reducing bacterial induced granulomatous inflammation in a mammal using agents that reduce B7-H1 expression or activity.
US8110682 Preparation and use of compounds as aspartyl protease inhibitors Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A is a bond, —C(O)—, or —C(R3′)(R4′)—; X is —N(R1)— or —C(R6)(R7)—; Y is —S(O)2—, —C(═O)—, —PO(OR9) or —C(R6′R7′)—; is a single or double bond and R, R1, R2, R3, R4, R3′, R4′, R5, R6, R6′, R7 and R7′ are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.
US7314926 Inhibiting cell proliferation, breast cancer, prostate cancer, cervical cancer, lung cancer, or tumor cells The present invention provides a method for inhibiting the proliferation of malignant and/or hyperplastic cells in a subject by administering to the subject a therapeutically effective amount of a guanosine rich oligonucleotide. The present invention also provides oligonucleotides which are capable of being specifically bound to a specific cellular protein which is nucleolin and/or nucleolin-like in nature, which is implicated in the proliferation of cells, specifically malignant and/or hyperplastic cells, and a method for their selection.
EP2271340B1 Pharmaceutical preparation comprising stephaglabrin sulfate for treating demyelinating diseases of the nervous system and for promoting restoration of the myelin sheath of nerve fibers The invention relates to a pharmaceutical remedy used to treat demyelinating diseases of the nervous system, said remedy containing stephaglabrin sulfate that contributes to the restoration of the myelin sheath of nerve fibers, and to a method for treating demyelinating diseases of the nervous system.
US20120004274 Use of inhibitors of jun n-terminal kinases to treat glaucoma Compositions and methods for lowering IOP and/or providing neuroprotection are disclosed. The compositions and methods are particularly directed to the use inhibitors of Jun N-terminal kinases (JNK) to lower IOP and/or provide neuroprotection.
CN102552265A Medicinal composition containing epigallocatechin gallate and camptothecin The invention belongs to the fields of medicine and gene engineering, and provides a composition for suppressing tumor cell proliferation. The composition for suppressing tumor cell proliferation comprises epigallocatechin gallate and camptothecin serving as active ingredients, and pharmaceutically-necessary auxiliary materials, wherein the molar ratio of the epigallocatechin gallate to the camptothecin is 8:1-0.5:1. As proved by experiments, the treatment effect of camptothecin on the suppression of tumor cell proliferation can be enhanced remarkably by using the composition prepared from the epigallocatechin gallate and the camptothecin or using the epigallocatechin gallate during dosing of the camptothecin. The composition basically has no toxicity on the liver and kidney of a nude mouse, the epigallocatechin gallate in the active ingredients has rich resources and low price, and the treatment cost of a tumor patient is reduced while the tumor suppression rate is increased simultaneously.
US20080009511 Cancer treatment with compounds inhibiting PKC alpha A chemotherapeutic cancer treatment with Gö7874, Gö6850, Gö7612, Gö7852, Ro31-7549, Ro31-8425, Ro31-8220, Ro31-0432 and NGIC-1 or chemical compounds with similar structures is administered to a mammal for the treatment of the cancer. The chemical compound is targeted to PKC α activity. Experiments indicate that Gö7874, Gö6850, Gö7612, Gö7852, Ro31-7549, Ro31-8425, Ro31-8220, Ro31-0432 and NGIC-1 and similar compounds to be effective for the treatment of breast cancer, leukemia, lung cancer, skin cancer, prostate cancer, liver cancer, brain tumor, cervical cancer, and cancers located in the digestive tract including gastric cancer and colorectal cancers. These treatments may be accomplished utilizing Gö7874, Gö6850, Gö7612, Gö7852, Ro31-7549, Ro31-8425, Ro31-8220, Ro31-0432 and NGIC-1 and chemical compounds with similar structures alone or in combination with prior art chemotherapy agents or with radiation therapy. In a preferred embodiment Gö7874, Gö6850, Gö7612, Gö7852, Ro31-7549, Ro31-8425, Ro31-8220, Ro31-0432 and NGIC-1 chemical compounds with similar structures is used for the treatment of cancer as a preventative drug by preventing cancer cell formation.
CN1565439A Osteoporosis relieving health food The invention relates to an Osteoporosis relieving health food which comprises at least calcium pyroracemic acid and soybean isoflavone, or other compatible additives, such as chondroitin sulfate calcium salt or Chitosan oligosaccharide or vitamins.
CN103735562A Ganoderma applanatum polysaccharide oral liquid and preparation method thereof The invention relates to a ganoderma applanatum polysaccharide preparation method, which comprises: mixing ganoderma applanatum polysaccharide powder, dehydrated alcohol and purified water according to a certain ratio, and completely and uniformly mixing the three materials to prepare the finished product. According to the present invention, the ganoderma applanatum powder is subjected to water boiling so as to extract part of the active polysaccharide component, then ethanol is adopted to further extract the active polysaccharide component, the precipitate obtained through centrifugation separation is washed through an organic solvent so as to remove the non-polysaccharide protein, and the product obtained through reduced pressure drying is the ganoderma applanatum polysaccharide powder, wherein with the process, the ganoderma applanatum polysaccharide powder yield is increased by 5-10%, the purity is increased by 2-5%, and the cost is reduced by 15-20%.
US20100226967 Imaging and therapeutic method using progenitor cells The invention relates to a method of treating or diagnosing a disease state worsened by progenitor cells. The method utilizes a composition comprising a conjugate or complex of the general formula Ab-X wherein the group Ab comprises a vitamin, or an analog thereof, that binds to progenitor cells, and when the conjugate is being used for treatment of the disease state, the group X comprises an antigen, a cytotoxin, or a compound capable of altering progenitor cell function, and when the conjugate is being used for diagnosing the disease state, the group X comprises a quantifiable marker.
WO2013146437A1 3-decenoic acid derivative and use for same [Problem] To provide a novel compound that is useful as an agent for preventing/treating cancer. [Solution] One aspect of the present invention provides a compound expressed by the chemical formula (1) or a pharmaceutically permissible salt thereof; the A in the chemical formula (1) is as defined in the specification. Furthermore, another aspect of the present invention pertains to a medicine containing the aforementioned compound or pharmaceutically permissible salt thereof as an active ingredient, as a use for the aforementioned compound. Yet another aspect of the present invention provides an agent for preventing and/or treating cancer, comprising the medicine.
WO2014146606A1 C-triaryl glucoside sglt-2 inhibitors The present invention relates to a C-triaryl glucoside SGLT-2 inhibitor shown as formula (I), preparation methods therefor, pharmaceutical compositions thereof and uses thereof for treating diseases that benefit from inhibiting SGLT-2. Such diseases are diabetes, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, delayed wound healing, insulin resistance, hyperglycemia, hyperinsulinemia, elevated blood level of fatty acids, elevated blood level of glycerol, hyperlipidemia, obesity, hypertriglyceridemia, Syndrome X, atherosclerosis or hypertension. The compounds of the present invention have strong inhibition activity against SGLT-2, higher selectivity, improved drug metabolism properties in oral treatment, and good druggability.
CA2312729C Use of 9-deoxy-2', 9-.alpha.-methano-3- oxa-4,5,6- trinor-3, 7-(1',3'-interphenylene) -13,14-dihydro- prostaglandin f1 to treat peripheral vascular disease An improved treatment for peripheral vascular disease is described using 9-deoxy-2', 9-.alpha.-methano-3- oxa-4,5,6- trinor-3, 7-(1',3'-interphenylene) -13,14-dihydro- prostaglandin F1.
US20080131523 Composition and therapeutic uses thereof A physiologically ingestible composition with microstructured water having a negative oxidation reduction potential of at least −40, and uses thereof are provided. The composition may further included dissolved oxygen, which may be present in an amount of 20 ppm to 150 ppm. The physiologically ingestible composition may be administered to reduce fatigue in a mammal.
CN102766068A Halogenated salicyloyl arylamine compounds as well as preparation method and application thereof The invention relates to the field of pharmaceutical chemistry, in particular to halogenated salicyloyl arylamine compounds (I) for oncotherapy, a preparation method of the compounds and medicine composites containing the compounds, wherein the definitions of Ar and R are defined in the specification. Pharmacological experiments prove that the compounds provided by the invention have excellent antitumor effect.
EP1592448A1 Use of a porphyrin compound for the treatment of skin fungi The present invention relates to the use of a photosensitizer compound with a specified structural formula for the treatment of a skin-borne fungus, a method of preparing a pharmaceutical composition for the treatment of a skin-borne fungus, and a method of treating a mammal suffering from a skin-borne fungus, such as Trichophyton rubrum.
WO2013093885A1 Inhibitors of notch signalling pathway and use thereof in treatment of cancers The present invention relates to use of inhibitors of Notch signalling pathway selected from the group consisting of 6-(4-Tert-Butylphenoxy)Pyridin-3-Amine (I3), its derivatives, in treating and/or preventing cancers.
US20100069443 Compound with benzamide skeleton having cyclooxygenase-1 (cox-1)-selective inhibitory activity This invention provides a novel COX-1-selective inhibitor. This invention relates to a novel compound represented by the formula below or a salt thereof. This invention also relates to an analgesic agent, an antiinflammatory agent, an antitumor agent, an antiplatelet aggregation agent, and a cyclooxygenase-1-selective inhibitor comprising, as an active ingredient, such compound or salt thereof.
CN103655641A Antrodia camphorata extraction method, antrodia camphorata oral liquid and preparation method of antrodia camphorata oral liquid The invention discloses an antrodia camphorata extraction method, antrodia camphorata oral liquid and a preparation method of the antrodia camphorata oral liquid. An antrodia camphorata extractive in the antrodia camphorata oral liquid is prepared by taking antrodia camphorata sporocarp or mycelium as an antrodia camphorata raw material. The antrodia camphorata oral liquid extracted from the antrodia camphorata sporocarp and mycelium tends to be natural. In order to extract effective components of the antrodia camphorata to a maximum extent, the antrodia camphorata extraction method comprises the steps of performing hot water extraction and ethanol extraction for the antrodia camphorata raw material in sequence, then processing extraction solutions obtained by the two steps, and adding the extraction solutions into the antrodia camphorata oral liquid according to a technical science. In order to improve medical effects of the antrodia camphorata, effective substances such as beta-glucan, fucoidin, arabinose, and the like are further added into the antrodia camphorata oral liquid and used for cooperating with the medical effects of the antrodia camphorata, so that the absorption rate and the effects of the antrodia camphorate oral liquid are maximized.
US20050203295 NO donor has a nitroso group attached to a tertiary carbon; vascular relaxants, nonsteroidal anti-inflammatory drug; water soluble; potentiated by adding glutathione, use low dosage A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group. In one embodiment, the C-nitroso compound is obtained by nitrosylation of a conventional drug or such drug modified to modify the carbon acid pKa thereof When such drug is a nonsteroidal anti-inflammatory drug, the resulting C-nitroso compound functions as a COX-1 and COX-2 inhibitor without the deleterious effects associated with COX-1 inhibition but with the advantageous effects associated with COX-1 and COX-2 inhibition. One such C-nitroso compound is a nitrosoketoibuprofen. A specific example of this kind of compound is isolated as dimeric 2-[4′-(α-nitroso)isobutyrylphenyl]propionic acid. In another case, the C-nitroso compound contains the moiety where X is S, O or NR. One embodiment is directed to COX-2 inhibitors where a tertiary carbon atom and/or an oxygen atom and/or a sulfur atom is nitrosylated.
EP1545539A2 Compositions for inducing increased levels of bgr-chemokines and methods of use therefor The present invention relates to compositions and methods for inducing increased levels and availability of β-chemokines by administering to a subject at least one G1 phase arresting compound, wherein the increased levels and availability of β-chemokines block chemokine/viral receptors thereby preventing or treating viral infections.
CN103127043A Stable and efficient dephosphorization composition The invention provides a stable and efficient composition for dephosphorization. The composition comprises lanthanum acetate hydrate and pharmaceutically acceptable proper auxiliary materials, wherein the average value of crystalline water in the lanthanum acetate hydrate is 0.5-8.0. The composition is applied in the form of oral administration, and the clinical daily dosage on the basis of anhydrous lanthanum acetate is 0.05-2.0g. The composition provided by the invention is free of aluminum and calcium, thereby avoiding the side effect of aluminosis, angiosteosis or the like of the patient due to taking of aluminum and calcium. The active component of the composition exists in the form of lanthanum acetate hydrate, so the solubility is high, and thus, the consistent high-level phosphorus combining capacity in vivo and in vitro can be always kept without being dependent on pH. The composition solves the problems of high consumption, high cost, poor mouthfeel and severe adverse reactions, including nausea, emesis and the like, in other lanthanum-containing dephosphorization medicines. The invention also provides a method for preparing the lanthanum acetate hydrate in the composition.
DE102006012319A1 Method for producing colored nanocorundum comprises mixing an aqueous solution of aluminum chlorohydrate with crystal nuclei and a precursor, drying by calcinations and agglomerating Method for producing colored nanocorundum comprises mixing an aqueous solution of aluminum chlorohydrate with crystal nuclei and a precursor of a coloring oxide former or a coloring oxide, drying by calcinations within less than 30 minutes and agglomerating the obtained product.
CN1765388A Quick-acting pain-alleviating broad-spectrum compound formulation Disclosed is a quick-acting pain-alleviating broad-spectrum compound formulation, which is prepared from cow-bezoar tablets, metronidazole, diclofenac sodium (diclofenac sodium), dexamethasone acetate and VB6.
EP1315473B1 Use of ectoine or ectoine derivatives for oral care The invention relates to the use of one or more compounds selected from compounds of formulae la and lb, the physiologically compatible salts of compounds of formula la and lb and the stereoisomer forms of compounds of formula La and lb, wherein R<1>, R<2>, R<3>, R<4> and n have the meaning cited in claim 1. Said compounds can be used advantageously in a preparation suitable for oral care.
US20130034522 Therapies for treating hepatitis c virus infection A method of improving the pharmacokinetics of VX-222 in a patient infected with HCV comprises co-administering VX-222 and VX-950 to the patient. A method of treating a patient infected with HCV comprises administering VX-222 and VX-950 to the patient, wherein VX-222 is in an amount of about 20 mg to about 400 mg, and wherein VX-950 is in an amount of about 100 mg to about 1,500 mg. A method of treating a patient infected with HCV comprises administering a therapeutically effective amount of VX-222, wherein VX-222 is administered at an amount of about 20 mg to about 2,000 mg once a day.
US7144882 Central nervous system disorders; psychological disorders; inflammatory bowel disorders This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.
CN1673225A Carbonate medicine precursors of hydroxycamptothecine and its derivative and their prepn and application The present invention discloses carbonate medicine precursors of hydroxycamptothecine and its derivatives as shown in expression I, II and III, their preparation process, stability in extracorporeal serum and enzyme and application in treating tumors.
CN101619089B Anticancer drug CL168, synthesis method and application thereof The invention discloses an anticancer drug CL168, a synthesis method and application thereof. Pharmacological experiments show that the compound has obvious anticancer effect, wherein the anticancer therapeutic index of CL168-6 is 49.3, and the compound can be used for preparing drugs capable of preventing and treating cancers such as liver cancer, lung cancer and the like and immunity diseases. In a structural formula I, when R represents O, CL-168-6R represents S, NH, SO2; in a structural formula II, R represents C2-C25 alkyl, aryl, substituted aryl of electron donor group or electron withdrawing group, C3-C6 alkynyl, alkenyl, C3-C9 naphthenic base, C3-C9 naphthenic base substituted by heteroatom, C1-C20 fatty acyl, aromatic acyl, sulfoyl, cinnamyl, galloyl, caffeoyl, benxoyl, feruloyl,L-aliphatic amino acyl, and L-aromatic amino acyl.
US20070249728 Synergistic Anti-Inflammatory Pharmaceutical Compositions and Methods of Use The invention provides a composition comprising a reduced isoalpha acid (RIAA) and isoalpha acid (IAA) isolated from hops, wherein the RIAA and IAA are in a ratio of about 3:1 to about 1:10. The invention also provides a method of reducing inflammation by administering a composition comprising a reduced isoalpha acid (RIAA) and isoalpha acid (IAA) isolated from hops, wherein the RIAA and IAA are in a ratio of about 3:1 to about 1:10.
CA2710713A1 Silencing of polo-like kinase expression using interfering rna The present invention provides compositions comprising interfering RNA (e.g., siRNA, aiRNA, miRNA) that target polo-like kinase 1(PLK-1) expression and methods of using such compositions to silence PLK-1 expression. More particularly, the present invention provides unmodified and chemically modified interfering RNA molecules which silence PLK-1 expression and methods of use thereof. The present invention also provides serum-stable nucleic acid-lipid particles (e.g., SNALP) comprising an interfering RNA molecule described herein, a cationic lipid, and a non-cationic lipid, which can further comprise a conjugated lipid that inhibits aggregation of particles. The present invention further provides methods of silencing PLK-1 gene expression by administering an interfering RNA molecule described herein to a mammalian subject. The present invention additionally provides methods of identifying and/or modifying PLK-1 interfering RNA having immunostimulatory properties. Methods for sensitizing a cell such as a cancer cell to the effects of a chemotherapy drug comprising sequentially delivering PLK-1 interfering RNA followed by the chemotherapy drug are also provided.
US20080045445 Modulating Notch1 Signaling Pathway for Treating Neuroendocrine Tumors Methods and pharmaceutical compositions for treating or suppressing symptoms of neuroendocrine (NE) tumors comprising increasing the levels or activities of Notch1 protein or other components of the Notch1 signaling pathway of the cancer cells. Also disclosed are pharmaceutical compositions for the methods.
CN102241657A Synthesis of isoflavone compound through Stille crossed coupling reaction The invention belongs to heterocyclic compound technical field, concretely relating to a heterocyclic compound in which unhydrogenated six-member heterocyclic ring containing an only ring hetero atom of an oxygen atom fuses with other phenyl rings. The invention provides a synthetic method of an isoflavone compound. The method comprises the steps of adding a reactant (substituted) 3-iodine chromone and tetraarylated tin into a solvent for a chemical reaction, and using column chromatography and recrystallization methods to purify the above resultant to obtain the pure compound of the present invention. By using the method, medicinal isoflavone such as daidzein, genistein, Ipriflavone, puerarin, formononetin and the like is prepared, and a new technical route of industrialization production of the above medicaments is established. Simultaneously, a series of novel isoflavone compounds with potential physiological activity are prepared.
WO2014052859A1 Pharmaceutical composition comprising benzyl alcohol for the treatment of migraines The present invention relates to intranasally administered pharmaceutical compositions for the treatment of headaches, such as migraines. Such pharmaceutical compositions comprise benzyl alcohol or a combination of benzyl alcohol and tetracaine. The invention also relates to methods for treating headaches, such as migraines, using these pharmaceutical compositions.
CN1833668A Medicinal compsns. having cooperative action A synergistic medical composition for preventing and treating diabetes and its complication, senile dementia, cardiovascular and cerebrovascular diseases, the thrombosis of central vein of retina, hyperlipemia, fatty liver, etc. features that it contains the extract(s) of natural plant(s).
EP1622600A1 Pharmaceutical formulation comprising anti-obesity agent and acidulant A pharmaceutical formulation comprising an anti-obesity agent, such as sibutramine, and at least one acidulant, such as fumaric acid, together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
WO2014145040A1 Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation Provided are cycloalkyl- and cycloalkenyl-substituted benzaldehydes and heteroaldehydes of formula (I) that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions containing the modulators, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from increased tissue oxygenation.
CN1820759A Tacrolimus solid dispersion and its preparing method The present invention belongs to the field of chemical medicine preparing technology, and is especially solid Tacrolimus dispersion as one kind of immunodepressant and its preparation process. The present invention adopts Tacrolimus as active medicine component, and prepares the solid Tacrolimus dispersion through adding carrier material, solvent process, solvent-fusing process and freeze drying process, and the solid Tacrolimus dispersion is further prepared into capasule. The present invention has raised medicine solubility, 5-500 times raised solubility in water compared with Tacrolimus, raised leaching speed and increased absorption of the medicine inside body.
US20090018102 Phamaceutical/cosmetic compositions comprising hyaluronic acid and treatment of dermatological conditions therewith Pharmaceutical/cosmetic compositions containing a dermatologically effective amount of hyaluronic acid, at least one retinoid and/or salt and/or derivative thereof, at least one oligosaccharide and at least one inhibitor of hyaluronic acid degradation, formulated into a physiologically acceptable medium therefor, are useful for the treatment of wrinkles, fine lines, fibroblast depletions and scars.
US7160914 Compounds that exhibit specific molecular recognition of mixed nucleic acid sequences and bind in the DNA minor groove as a dimer Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.
US7645743 Administering immunity linkers with more than one binding site, wherein second site binds to target and individual has pre-existing cellular or humoral immune response to first site; high speed response to public health needs such as pandemic infections; biological warfare; vaccines Methods and compositions for immediately immunizing an individual against any molecule or compound. The present invention comprises an immunity linker with at least two sites; (1) at least one first binding site that binds to an immune response component in an individual that has been pre-immunized with a universal immunogen, and (2) at least one second binding site that binds specifically to a desired compound or molecule, the target.
WO2004084874A3 Mtp inhibitors for inhibiting inflammation The invention provides a method of inhibiting inflammation such as hepatitis or colitis in a mammal, by administering to the mammal composition containing a compound which inhibits the expression or activity of a microsomal triglyceride transfer protein.
US20120232030 Heat stable hyaluronic acid compositions for dermatological use The disclosure provides hyaluronic acid (HA) gel formulations and methods for treating the appearance of the skin. The formulations hyaluronic acid and at least one additional ingredient. Methods for treating lines, wrinkles, fibroblast depletions, and scars with the disclosed composition are provided as well.
US8084049 Complexes of fatty acid esters of polyhydroxyalkanes and pyridine carboxy derivatives The present invention relates to novel combinations of fatty acid derivatives and pyridine carboxy derivatives, including fatty acid esters with glycerol and 3-carboxy pyridine derivatives such as niacinamide. Such combinations have surprisingly shown antiviral and anti-microbial activity and the use for the treatment of inflammatory conditions and infections is disclosed herein.
WO2014059220A1 Glycosphingolipids and methods of use thereof The invention provides, inter alia, immunoinhibitory glycosphingolipids and immunoinhibitory alpha-galactosylceramides and compositions and preparations thereof, and methods of use thereof including in the treatment of conditions characterized by increased iNKT cells and/or activity.
WO2010050179A1 Prophylactic/ameliorating agent for adult diseases comprising 5-aminolevulinic acid, derivative of 5-aminolevulinic acid, or salt of 5-aminolevulinic acid or the derivative of 5-aminolevulinic acid as active ingredient Disclosed are: a pharmaceutical composition of which the mechanism of action relies on the improvement in basal metabolism unlike conventional biochemical reaction inhibition type of therapeutic agents for adult diseases, and which has no adverse side effect, and against which no drug resistance is caused for adult diseases; and a method for preventing/treating adult diseases using the pharmaceutical composition. Specifically disclosed are: a prophylactic/ameliorating composition for adult diseases such as metabolic syndrome, diabetes, hyperlipidemia, hypertension, hepatic function disorders, renal failure, obesity, erectile dysfunction, climacteric disorders, shoulder stiffness and lumbago, which comprises 5-aminolevulinic acid (ALA), a derivative of ALA, or salt of ALA or the derivative of ALA, preferably ALA, a derivative of ALA, or salt of ALA or the derivative of ALA and an iron compound such as sodium ferrous citrate, sodium ferric citrate and ammonium ferric citrate; a food or a food material for preventing/ameliorating adult diseases, which contains the composition; a method for utilizing the composition for the preparation of a prophylactic/ameliorating agent for adult diseases; and others.
CN101244056A Combination capable of preventing prostate gland cancer The invention relates to a composition for preventing prostatic cancer, comprising lycopene, vitamin B1, vitamin B2, vitamin B3, vitamin B6, vitamin B12, vitamin C, caffeine, epicatechin, ECG, epigallocatechin, epigallocatechin gallate (EGCG), quercetin and vitamin E. The composition has the advantages of having obvious preventing, reversing or deferring functions for prostatic cancer and reducing the incidence of cancer.
WO2009128918A1 Combination therapy using a soluble hyaluronidase and a bisphosphonate Provided are combinations, compositions and kits containing a bisphosphonate composition and a soluble hyaluronidase composition formulated for subcutaneous administration. Such products can be used in methods of treating bisphosphonate- treatable diseases or conditions. Also provided are methods for subcutaneous administration of a bisphosphonate compound whereby the dosing regimen is substantially the same as for intravenous administration of the same dosage for treatment of the same bisphosphonate-treatable disease or condition.
CN1899389A Medicinal composition for preventing and treating female senile diseases and method for preparing said preparation The present invention relates to a kind of medicinal composition for preventing and treating female senile diseases and its preparation process. The medicinal composition consists of isoflavone, panoxadiol type saponin, cimicifuga rhizome extract and calendic acid. It has high stability, and can replenish female with paraestrogen to prevent diseases caused by estrogen decrease, improve senility symptoms, nurse skin, resist oxidation and eliminate the accumulation of free radical and other toxic matters.
CN1565473A Water soluble nightshade extract, its preparation method and pharmaceutical compositions The invention provides a water-soluble extract originated from eggplant genus plant, which substantially comprises 60-90% of Solasonine and solamargine, the invention also discloses a process for preparing the water-soluble extract of the eggplant genus plant, and a medicinal composition containing the water-soluble extract.
US20110306605 Coumarin-based compounds for the treatment of alzheimer's disease and cancer Compounds including those of the Formula I where X, R1, R2 and subscript t are as defined herein, useful as γ-secretase inhibitors, are provided, as are compositions comprising the compounds, as well as methods for use of the compounds for treating or preventing neurodegenerative diseases, such as, for instance, Alzheimer's disease.
US20120149662 Heterocyclic Compounds as Janus Kinase Inhibitors The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula (I).
WO2012118915A2 Compositions and methods for treatment of tamoxifen resistant breast cancer The inventors found that the gene, HOXB7, was frequently overexpressed in breast cancer, and is a major upstream regulator of events leading to tamoxifen resistance. The present invention provides double-stranded short interfering nucleic acid (siNA) molecules that targets the HOXB7 gene in cells, and also provides methods of use of this siNA molecule for methods of screening, diagnosis and prediction of treatment outcomes as well as treatment of cancer.
CN101759692A Preparation and use of thiocarbonyl compound The invention belongs to the field of anti-tumor relative medicine, and provides a thiocarbonyl isoxazoline derivative comprising a structure represented by general formula I and pharmaceutically acceptable salt thereof; in the formula, R stands for FORMULA. The invention further provides use of the compound or pharmaceutically acceptable salt thereof as medicine, specifically as anti-tumor medicine.
US20110208118 Compositions and means for treating uterine leiomyomata, leiomyoma, myoma, uterine fibroids, endometriosis, adenomyosis and related disorders by mifepristone The present invention provides a vaginally administrable tablet useful for treating leiomyomata, leiomyoma, myoma, uterine fibroids, endometriosis, adenomyosis and other related disorders. The tablet comprises mifepristone, at least one non-effervescent excipient or diluent, and at least one effervescent excipient.
US20110014289 Reticulated Elastomeric Matrices, Their Manufacture and Use in Implantable Devices This invention relates to biodurable, reticulated elastomeric matrices that are resiliently-compressible, their manufacture and uses including uses for implantable devices into or for topical treatment of patients, such as humans and other animals, for therapeutic, nutritional, or other useful purposes.
WO2010089391A1 New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders The present invention provides pharmaceutical compositions comprising one or more CRTH2 antagonists1 and one or more further active compounds 2.
CA2377126C Thiazole and oxazole derivatives and their pharmaceutical use Compounds of Formula (I) are disclosed. These compounds include selective activators of human PPAR delta.
US20080261971 Novel Heterocyclic Nf-Kb Inhibitors The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, (II) or (III) R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1; q is 0, or 1; X is CO, or SO2.
EP1153034B1 Growth hormone secretagogues What is disclosed are growth hormone secretagogues, and their uses, of formula (I) wherein R1 is C6H5CH2OCH2-, C6H5(CH2)3- or indol-3-ylmethyl; Y is pyrrolidin-1-yl, 4-C1-C6 alkylpiperidin-1-yl or NR2R2; R2 are each independently a C1 to C6 alkyl; R3 is 2-napthyl or phenyl para-substituted by W; W is H, F, CF3, C1-C6 alkoxy or phenyl; and R4 is H or CH3, or a pharmaceutically acceptable salt or solvate thereof.
US20080269287 Substituted Pyridone Derivative Compounds of a formula (I) [wherein, A represents formula (III-1) R3 is a hydrogen, lower alkyl et al; m is 0 or 1; R1 is a hydrogen atom, halogen atom et al, R2 is a hydrogen et al; p is 0 to 4; X is a carbon atom or nitrogen atom; and X1 to X4 is a lower alkyl et al], or pharmaceutical acceptable salts thereof. These have a potency antagonistic to binding to histamine H3 receptor, or have a potency inhibiting the constant activity of histamine H3 receptor, and are useful in the therapy of obesity, diabetes et al.
WO2013050625A8 Antiviral efficacy of disodium 2,6-dimethyl-1,4-dihydropyridine-3,5-bis(carbonyloxyacetate) and its derivatives Antiviral efficacy of disodium 2,6-dimethyl-1,4-dihydropyridine-3,5- bis(carbonyloxyacetate) and its derivatives (compound with general formula I) wherein R is hydrogen, methyl or ethyl.
US20120157917 High pressure delivery system and method for treating pelvic disorder using large molecule therapeutics The invention relates generally to methods and systems for the treatment of pelvic tissues using a high pressure injection device to deliver a therapeutic composition that includes a large molecule therapeutic agent, such as a nucleic acid or a polypeptide, to a target tissue in the pelvic area. Methods of the invention can improve delivery of the therapeutic agent into the tissue, which can be beneficial for the treatment of a pelvic tissue disorder, such as bladder and prostate tumors.
US7438899 Gastrointestinal disorders; anticancer agents; sustained release The present invention relates to the treatment of gastrointestinal disease and/or cancer, and a method of weight gain, via the ingestion of polymeric compositions in humans, animals or birds in need of said treatment. The invention provides methods for the treatment of cancer, the treatment and/or prevention of gastrointestinal disease and/or infection and/or diarrhoea, and a method for increasing weight gain in humans, animals or birds comprising administering to said humans, animals or birds an effective amount of a pharmaceutical or veterinary composition, or feed additive, comprising an effective amount of a polymer and/or copolymer, having the repeating polymeric unit (I), wherein R is H or alkyl, usually C1 to C4, or this unit in hydrated, hemiacetal or acetal form, together with a pharmaceutically or veterinarally acceptable carrier, diluent, adjuvant, excipient and/or controlled release system.
WO2006056874A1 Salt form The present invention provides the benzenesulphonate salt of (1α,3α,5α)-[3-(aminomethyl)bicyclo[3.2.0]hept-3-yl]acetic acid which has the following structural formula (II).This compound is particularly suitable as a drug substance and is useful in the treatment of pain, epilepsy and other conditions.
WO2013117137A1 Lupane triterpenoid derivatives and pharmaceutical use thereof Disclosed are lupane triterpenoid derivatives and pharmaceutical use thereof, specifically lupane triterpenoid derivatives of formulae (I)~(III), a pharmaceutical composition and a combination preparation comprising said lupane triterpenoid derivatives or a pharmaceutically acceptable salt thereof in a therapeutically-effective dose, particularly the use in preparation of a medicament for the treatment of HIV-1/AIDS.
US20080050378 A ribonucleotide sequence corresponding to a gene KIF11 target sequence, where the antisense strand comprises a ribonucleotide sequence complementary to the sense strand; sense/anntisense strands hybridize to form double-stranded molecule which inhibits cell expression of KIf11 (SEQ ID NO: 34) Disclosed are methods for detecting non-small cell lung cancer (NSCLC) using differentially expressed genes KIF11, GHSR1b, NTSR1, and FOXM1. Also disclosed are methods of identifying compounds for treating and preventing NSCLC, based on the interaction between KOC1 and KIF11, or NMU and GHSR1b or NTSR1.
WO2012145119A3 Low inflammatory blended oils A low inflammatory oil composition and method for supplementing feed, nutrition and diet systems with omega-3 to omega-6 balanced oils comprised of a synergistic blend of at least two oils. The composition further comprises a synergistic blend of long chain omega-3 oil as a means to further increase the nutritional value. The composition further provides an effective increase in reducing inflammation for therapeutic, and pharmacological treatment in addition to general nutrition and diet systems.
CN101041640A Antineoplastic active substance of diketopiperazine PJ147and PJ157 The invention discloses two tumour-proof active material PJ 147 and PJ 157, which is characterized by the following: gathering acetone extract of Gliocladium sp.YUP08 mycelium as raw material to separate through chromatogram method; obtaining the compound with the following structural formula; fermenting the Gliocladium sp to obtain large amount of ferment liquid; filtering; obtaining mycelium and water layer; drying the mycelium in the bottle; extracting acetone through ultrasound; decompressing to recycle solvent without residule; drying; dissolving through carbinol repeatingly; obtaining dissolvable concrete of carbinol; dissolving mycelium extract through acetone; separating through silicon sol column chromatogram; proceeding gradient elution through ligarine-acetone; obtaining each fraction as the product; fitting for preparing tumour-proof drug.
WO2007111227A1 Acylaminopiperidine compound [PROBLEMS] To provide a compound that exhibits excellent CCR4 or TARC and/or MDC function regulating activities and can be used in prevention and/or therapy for various inflammatory diseases, allergic diseases, autoimmune diseases, etc. [MEANS FOR SOLVING PROBLEMS] Acylaminopiperidine compounds of the formula (I) or pharmaceutically acceptable salts thereof. (I) In the formula, the characters have the following meaning. A: single bond or C1-C6 alkylene. R1: optionally substituted phenyl, etc. R2: -H or C1-C6 alkyl. R3: -H, C1-C6 alkyl or C3-C8 cycloalkyl. R4: optionally substituted pyrrolidin-2-yl, etc. D: benzene ring or pyrazole ring.
WO2011030103A1 Screening method and therapy with agonists of ddah i The present invention derives from the finding that decreased levels of DDAH I are associated with increased portal pressure and that by increasing DDAH I levels in vivo, portal pressure may be reduced. Accordingly, the invention provides methods for reducing portal blood pressure comprising administering to a subject in need thereof an agonist of DDAH I.
US20110268786 Patch production technology The invention relates to a transdermal, especially dopaminergic patch, comprising a release liner film, an active substance layer, and a carrier film, wherein the active substance layer is applied between the release liner film and the carrier film. The release liner film and/or the carrier film thereby comprise at least one separation edge brought about thermally, at least partially defining a peripheral edge of the patch. The invention further relates to a method for producing such a transdermal patch and to a tool for producing the patch according to the method according to the invention. Crystal growth in the active substance layer can be reliably prevented by the patch according to the invention.
CN102134220A 9-amsacrine derivatives as well as preparation method and application thereof The invention discloses 9-amsacrine derivatives as well as a preparation method and application thereof and particularly discloses acridine derivatives with multi-target protein kinase inhibition activity as well as a preparation method and application thereof. The structural formula of the acridine derivatives is shown in a formula I, wherein X1-X3 are C, or one of X1-X3 is N, and the other two of X1-X3 are C; R1-R5 are selected from the following substituted groups: H, OH, OCH3, OC2H5, F, Cl, Br, CH3, CF3, OCF3, NH2, COOH and NHCOCH3; R6-R13 are selected from the following substituted groups: H, F, Cl, Br, OCH3, COOH, CH3, NO2, NHCOCH3 and CF3; R7 and R11 are preferably selected from Cl and OCH3; and Z is selected from NH and NHCH2. An in vitro cell proliferation experiment indicates that the compound shown in the formula I can well inhibit the proliferation of leukemia cell K562. An in vitro protein kinase inhibition experiment shows that the compound shown in the formula I is a multiple target protein kinase inhibitor. The formula I is shown in the specification.
US20100062000 Rhamm, a Co-Receptor and Its Interactions with Other Receptors in Cancer Cell Motility and the Identification of Cancer Prognitor Cell Populations CD44 is an integral hyaluronan receptor that can either promote or inhibit motogenic signaling in tumor cells. Rhamm is a non-integral cell surface (CD168) and intracellular hyaluronan binding protein that promotes cell motility in vitro and whose expression is strongly upregulated in aggressive tumors. The present invention describes compositions and methods for the prognosis and diagnosis of cancer by the detection of CD44/Rhamm complexes. The use of labeled Rhamm-binding agents in culture and in vivo to identify tumorigenic progenitor cells that exhibit an aggressive phenotype characterized by high Rhamm and CD44 expression is further described. Specific methods include using hyaluronan to target imaging or therapeutic agents to these progenitor tumor subsets in breast and likely other cancers.
CA2354770C Compositions with enhanced photoprotective effect and method for using same The present invention relates to a sunscreen composition for topical application to the skin comprising a fluororesin having a submicron in combination with a sunscreen agent and an oil component. These compositions provide a boost in the SPF value of the composition.The invention also provides methods relating to the use of these compositions for boosting the SPF and decreasing the irritation on the skin caused by imitating sunscreen agents.
WO2009151762A2 Anticancer methods using extracts of anemarrhena asphodeloides bunge Selective apoptotic extracts of Anemarrhena asphodeloides Bunge are provided. Also provided are methods of using said extracts to induce apoptosis in specific cells, especially in a human. Provided as well are uses of the extracts of Anemarrhena asphodeloides Bunge for the preparation of a medicament for the selective induction of apoptosis in a living being.
CN102089283A Glucocorticoid receptor agonist composed of 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative having substituted oxy group Disclosed is a glucocorticoid receptor agonist composed of a compound represented by formula (1) or a salt thereof, which is a 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative having a substituted oxy group. A novel pharmacological action of the agonist is also disclosed. In the formula, R1 represents a group represented by formula (2a), (3a), (4a) or (5a); R2 represents -(CO)-R8, -(CO)O-R9 or the like; R2-O- is substituted at the 4-position or the 5-position of the benzene ring A; R3 represents a lower alkyl group; R4, R5, R6 or R7 represents a halogen atom, an optionally substituted lower alkyl group or the like; m, n, p or q represents 0, 1 or the like; and R8, R9 or the like represents an optionally substituted lower alkyl group, a lower alkenyl group or the like.
WO2005077359A1 Stabilized pharmaceutical composition containing indoline compound Disclosed is a pharmaceutical composition containing N-(1-octyl-5-carboxymethyl-4,6-dimethylindoline-7-yl)-2,2- dimethylpropane amide or a pharmacologically acceptable salt thereof, which also contains a pharmacologically acceptable antioxidant, acidic compound or a mixture of them as a stabilizer.
CN103341154A Compound veterinary injection for clearing heat and removing toxin The invention discloses a veterinary injection for clearing heat and removing toxin, relating to the technical field of veterinary preparations. Every 10ml of the injection comprises the following raw material medicines in percentage by mass: 0.10-1.00% of honeysuckle extract based on chlorogenic acid, 1.00-5.00% of scutellaria baicalensis extract based on scutellaria baicalensis, 0.20-1.00% of amoxicillin, 0.80-1.20% of benzyl alcohol and 40,000-80,000 units of antibacterial peptide; the pH is adjusted to 4.0-8.0; and injection water is added to the full dose. The injection disclosed by the invention is mainly used for treating the influenza and respiratory diseases of livestock and poultry and is safe and reliable without any toxic and side effect and residue; and by adopting an injection method for administration, the bioavailability of the medicine is high, the medicine takes effect quickly, the curative effect is good, and the veterinary injection is convenient to use.
WO2008053158A1 Inhibitors of p38 mitogen-activated protein kinase Compounds of formula (I) are inhibitors of p38 MAP kinase activity, and are useful in the treatment of, inter alia, inflammatory and autoimmune disease formula (I): wherein R3, R4, R5 and R6 are each independently hydrogen or halogen; M and P are independently -N= or -CH=; Z is (a) a radical of formula R1R2CHNH-Y-L1-X1-(CH2)Z-, wherein R1R2CHNH- is an N-linked amino acid or amino acid ester group as defined in the description, and -Y-L1-X1-(CH2)Z- is a linker radical as defined in the description.
US8703752 Use of mifepristone and derivatives therefor as Hedgehog protein signaling pathway modulators and applications of same The invention relates to a novel use of compounds having formula (I), including mifepristone (RU 486 or RU 38 486) and the derivative salts thereof, for the preparation of a medicament that can modulate (activate or inhibit) the Hedgehog protein signalling pathway, which is intended for the treatment of pathologies involving a tissue dysfunction linked to deregulation of said pathway.
CA2277951C Imino-aza-anthracyclinone derivatives A compound of formula (1), wherein R1 and R2 are independently selected from hydrogen and an organic residue, and R3 is a group of the formula OR6 or NR7R8, or a pharmaceutically acceptable salt thereon, is useful in the treatment of amyloidosis.
US20080096962 tert-Butyl 2-{2-[1-ethyl-3-(4-trifluoromethoxy-phenyl)-ureido]-indan-5-ylsulfanyl}-2-methyl-propionate; peroximose proliferator activated receptor antagonist; cardiovascular desease, diabetes; coupling N(5mercapto-indan-2yl)acetamide with (2methyl-2halo) propionate and 2-(4-hydroxyphenoxy)propionic acid The present invention relates to novel processes for the preparation of substituted tetralin and substituted indane derivatives. The present invention is further directed to novel processes for the preparation of intermediates in the preparation of the substituted tetralin and substituted indane derivatives.
US20080286354 administering a bile acid e.g ursodiol, ursodiol bicarbonate and ursodiol sulfate, a fibrate e.g. bezafibrate, fenofibrate, gemfibrozil, ciprofibrate and derivatives of 2-phenoxy-2-methylpropanoic acid, and a statin e.g. simvastatin, fluvastatin, pravastatin, atorvastatin to treat chronic hepatitis The invention relates to pharmaceutical compositions comprising at least one fibrate and at least one bile acid, and to methods for the treatment of hyperlipidaemia or elevated liver function tests in a patient by administering at least one fibrate and at least one bile acid to the patient.
CN102526084A Roxithromycin ambroxol tablet The invention provides a roxithromycin ambroxol tablet, which consists of the following components in parts by weight: 150 parts of roxithromycin, 30 parts of ambroxol hydrochloride, 60 parts of microcrystalline cellulose, 20 parts of sodium starch glycolate, 6 parts of poloxamer, an appropriate amount of bonding agent and optionally existing flow aid and lubricating agent. In the invention, the roxithromycin ambroxol tablet is prepared by adopting specified auxiliary materials and auxiliary material proportion, and particularly, microcrystalline cellulose, carboxyrnethyl starch sodium and poloxamer are taken as a filler, a disintegrating and a solubilizer, so that the using amount of the auxiliary materials is greatly reduced, cost is greatly lowered, the tablet weight is light, convenience is brought to taking, the dissolution of active ingredients is ensured, and the bioavailability is increased. The roxithromycin ambroxol tablet has remarkable advantages.
CN101054400A Novel Panoxadiol and derivative, preparation method and medical use thereof The present invention relates to panaxadiol and its derivative, its preparation method and medicinal uses, belongs to natural medicine field, more specificly relating to dammar-20-(22)-ene-3 beta, 12 beta,25-triol. The molecular formula is : C30H52O3. The molecular weight is 460. The panaxadiol and its derivative preparation method comprise acid degradation preparation method and alkaline degradation preparation method and purification step. The acid degration of ginseng root general ginsenoside proceed in organic solvent acid aqueous solution containing protecting agent, while the alkaline degration of ginseng root general ginsenoside proceed in organic solvent acid aqueous solution. The present invention also relates to uses of the panaxadiol in preparing assistant drug for treating senile dementia, cerebral vascular dementia and tumour treatment. The beneficial effect : the drug prepared from panaxadiol has obvious curative effect for treating senile dementia, cerebral vascular dementia and tumour treatment.
WO2014125084A1 Hydroxyindalpine derivatives and their medical use The present invention relates to hydroxyindalpine derivatives of formula (I) as defined herein and pharmaceutical compositions comprising these compounds, as well as their medical use, particularly in the treatment or prevention of gastrointestinal diseases/disorders, such as constipation and functional dyspepsia.
CN102240261A Preparation method and medicinal purpose of glucomannan injection The invention discloses a preparation method and a medicinal purpose of a glucomannan injection. According to the method, the injection is prepared through treating glucomannan with high purity, good homogeneity and a specific molecular weight (10-100 kDa) as a raw material, adding an electrolyte salt for adjusting the osmotic pressure as needed, carrying out proper technical processing, packaging, and processing with a proper disinfection process. The invention simultaneously discloses the new medicinal purpose of the glucomannan injection in blood volume supplement aspects. The preparation method of the invention which has the advantages of simple operation, easy control, industrial production and the like is suitable for preparing natural source glucomannan (such as polysaccharides, konjac gel and the like) injections; and the glucomannan injection with different molecular weight specifications which has different half lives in organisms can satisfy corresponding medicinal requirements.
WO2008154347A1 Spirobenzoazepines as vasopressin antagonists The present invention is directed to a compound of Formula (I) or a form thereof: wherein U, V, W and Ring A are as defined herein, useful as vasopressin receptor antagonists.
CN1969833A Dry powder composition containing CoQ10 and preparation process thereof The invention discloses a dry powder composition with coenzyme Q10 and preparing method, which comprises the following parts: 1%-60% active coenzyme Q10, 10%-70% excipient, 10%-80% clad wall material, 1%-15% antioxidant and water.
WO2007102438A1 Fractionation product of aqueous extract of eucommia ulmoides oliver leaf, and anti-obesity agent comprising the fractionation product [PROBLEMS] To provide: a fractionation method for extracting an ingredient, particularly a pharmacologically active ingredient such as an iridoid compound, from an Eucommia ulmoides oliver leaf with good efficiency; a fractionation product of an Eucommia ulmoides oliver leaf, wherein the fractionation product contains a specific component in a large concentration; and an anti-obesity agent, composition for oral ingestion, pharmaceutical composition, food composition, pharmaceutical or food which comprises a natural material as a raw material, produces little adverse side effects, and is safe even when ingested over a long period. [MEANS FOR SOLVING PROBLEMS] Disclosed is a fractionation product of an aqueous extract of an Eucommia ulmoides oliver leaf. The fractionation product can be produced by: adsorbing an aqueous extract of an Eucommia ulmoides oliver leaf onto a reverse-phase synthetic adsorbent, wherein the aqueous extract is prepared from a dried Eucommia ulmoides oliver leaf; washing the adsorbent with water; and eluting the fractionation product with a 5-80 vol% aqueous methanol solution. Also disclosed is a pharmaceutical or food having an anti-obesity activity, which comprises the fractionation product.
US20110293693 Quantum unit of inheritance vector therapy The innovative treatment strategy described here utilizes configurable microscopic medical payload delivery devices to act as a transport vector to deliver quantum genes to specific type of cells in the body. Utilizing probes on the exterior of the transport device, transport device locate specific target cell types in the body. Once a specific target cell type has been encountered, the configurable microscopic medical payload delivery device inserts its payload of quantum genes into the target cell type. By delivering quantum genes to specific type of cells, genes can be activated or inactivated in those specific type of cells. These medically therapeutic quantum genes are intended to improve cell function or the longevity of cells or neutralize harmful cells that pose a hazard to the general health of the body.
EP2401267A1 Jak kinase modulating quinazoline derivatives and methods of use thereof Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. (I).
US20070275908 Methods and Compositions for the Enzymatic Synthesis of Gangliosides Novel synthetic glycosphingolipids and pharmaceutical compositions containing such synthetic glycosphingolipids are described. Methods of making the novel synthetic glycosphingolipid compounds and compositions as well as their use in the field of neuroprotection and cancer treatment is also described.
WO2008092844A1 Piperidin-acetamide derivatives for the treatment of inflammatory or allergic diseases A compound of formula (I), wherein substituents are as given above, useful in the treatment of a disease mediated by the action of CCR3, wherein R1 and R2 independently are (C6-18)aryl or (C6-18)aryl(C1-6)alkyl one or morefold substituted by (C1-6)alkyl, C(1-6)aIkoxy, halo(C1-6)alkyl, halogen or unsubstituted or substituted heterocyclyl having 5 or 6 ring members and 1 to 4 heteroatoms selected from N, O, S.
US8450309 Arthroscopic irrigation solution and method for peripheral vasoconstriction and inhibition of pain and inflammation A method and solution for perioperatively inhibiting a variety of pain and inflammation processes during arthroscopic procedures. The solution preferably includes a vasoconstrictor that exhibits alpha-adrenergic activity and one or more additional pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for peripheral vasoconstriction and inhibition of pain and/or inflammation while avoiding undesirable side effects associated with systemic application of larger doses of the agents.
CN1579463A Compound cape-jasmine salted-fermented beans total extract and its preparation and use The invention relates to a compound gardenia extract and its manufacturing method, the invention also relates to the medicine compound containing the extract. The invention uses solution extraction method, solution extraction method, and resin absorbing method or several methods together of them, and the extract is processed into oral medicine or external medicine such as injection solution and external solution: powder, particle, tablet, capsule, pill, and so on. The invention can be applied to cure climacteric syndrome, osteoporosis, hyperlipemia, and preventing cancer, it also has functions for insomnia, hepatits, coronary heart disease, stomack hemorrhage, spirit system disease, and so on.
CN101612138B Cefetamet pivoxil hydrochloride capsule and preparation method thereof The invention relates to a cefetamet pivoxil hydrochloride capsule which contains the raw materials by the weight percent: 59% of effective and active ingredient, 10-15% of disintegrant, 1-3% of solubilizer, 20-28% of bulking agent and 2-3% of lubricating agent; wherein the effective and active ingredient is cefetamet pivoxil hydrochloride; the disintegrant comprises sodium carboxymethyl starch and cross-linked sodium carboxyl cellulose; the solubilizer is lauryl sodium sulfate; the bulking agent is one or two of lactose and mannitol; and the lubricating agent includes superfine silica powderand magnesium stearate. The invention also discloses a preparation method of the cefetamet pivoxil hydrochloride capsule, which adopts dry pressing pelletization technique; therefore, the invention has the advantages of simple equipment and less investment; the prepared capsule is stable in quality, excellent in solubility property, rapid in absorption, convenient in taking and good in mouthfeel.
CN102327213A Triamcinolone acetonaide acetate nano eye drops and preparation method thereof The invention relates to triamcinolone acetonaide acetate nano eye drops and a preparation method thereof, wherein the triamcinolone acetonaide acetate nano eye drops are prepared in the way that the triamcinolone acetonaide acetate and the chitosan nano carrier are prepared into nanoparticles according to the proportion of 1/2 and then are mixed with the distilled water. The invention provides the triamcinolone acetonaide acetate nano eye drops which have simple preparation process, can prevent pain and complication which are caused by local injection, facilitate clinical use and are easy to be accepted by patients and the preparation method of the triamcinolone acetonaide acetate nano eye drops.
CN101322848B Composition for gastroscopy and preparation thereof The invention relates to a combination drug used in the gastroscopy, in particular to a combination drug comprising dimethicone emulsion or simethicone emulsion and analgesics or local anesthetics and a preparation method thereof. The combination drug is mainly prepared by the following raw materials of 0.1-5wt percent of analgesics or local anesthetics, 1-40wt percent of dimethicone emulsion/simethicone emulsion, 0.1-8wt percent of emulsifier, 0-20wt percent of thickening agent, 0.01-0.5wt percent of antibacterial agent and 27-98wt percent of pure water. Compared with the prior art, in the preparation of the invention, the dimethicone emulsion/the simethicone emulsion is scattered and emulsified into liquid drops which have the particle size of about 300nm, has large specific surface area, short defoaming time and good effects; liquid drops with the nano size scattered and emulsified by the dimethicone emulsion/the simethicone emulsion have good stability without oil leak, dispersion, and the like, when in storage for a long term.
US20090162429 Slow-Release Composition, Method for the Preparation Thereof, and Use Thereof The pharmaceutical or nutraceutical composition with sustained release of an active ingredient according to the present invention comprises at least one coated granule; the coated granule being composed of a particle that comprises said active ingredient and is coated with at least two coatings that comprise a combination of excipients. The present invention relates also to a process for the preparation of the composition.
US20050180965 Heat-reversible composition treating hyposalia and asialia A heat-reversible composition designed to compensate salivary deficiencies, includes at least a polymeric compound whose viscosity is low at room temperature and which increases at oral temperature so as to reach optimal viscosity at oral temperature to gelling point.
US8008322 Substituted pyrazolopyridines, compositions containing them, method for the production thereof, and their use The disclosure relates to substituted pyrazolo-pyridines, compositions containing them, methods for the production thereof, and to their use as medicaments, in particular, as anticancer agents.
CN102106817A Pre-emulsified propylgallate concentrate and preparation thereof The invention discloses pre-emulsified propylgallate concentrate for treating cardiovascular diseases as well as the preparation method and pharmaceutical application thereof. The pre-emulsified concentrate comprises propylgallate, oil phase, surfactant, latent solvent, and the like and is used for treating ischemic cerebrovascular diseases such as acute cerebral infarction, chronic cerebral thrombosis, lacunar cerebral infarction and cerebral vascular insufficiency as well as brain coma sequela, cerebral trauma, cerebral concussion, coronary heart disease, angina pectoris, hypertension, congestive heart failure, pulmonary heart disease and peripheral angiopathies such as thrombophlebitis, and the like.
WO2012061012A3 4-amino-2h-pyran-2-one analogs as anticancer agents Compounds of Formula I are described, along with methods of using such compounds for the treatment of cancer and pharmaceutical formulations thereof.
CN103003250A Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k The invention provides novel bicyclic azaheterocyciic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
US20090117195 Hydrophilic Particles Based on Cationic Chitosan Derivatives The present invention provides new nanoparticles and microparticles of hydrophilic character, prepared out of a cationic chitosan derivative and a polyanionic polymer.
WO2008120966A1 Pharmaceutical composition in the form of a sublingual tablet consisting of a non-steroidal anti-inflammatory agent and an opiate analgesic for pain management The invention relates to a pharmaceutical composition consisting of a combination of two active ingredients, one of said active ingredients being a non-steroidal anti-inflammatory agent, known as ketorolac, and the other being an opiate analgesic known as tramadol. Said agents are formulated in the form of an orally administered sublingual tablet used to relieve and/or treat moderately or severely intense pain. The combination of said pharmaceuticals generates a stronger analgesic effect, greater bioavailability and a faster speed of action using smaller dosages, with less collateral effects.
WO2014038881A2 Protein kinase inhibitor comprising pyridine derivatives The compound according to the present invention and the pharmaceutically acceptable salts thereof inhibit the activity of protein kinase, and therefore, can be effectively used in preventing or treating diseases relating to the activity of protein kinase.
EP2624840A1 New treatments of hepatitis c virus infection The invention concerns the use of cyclophilin inhibitors in the treatment of Hepatitis C virus genotype 2 or 3 infection.
US20100249085 Heteroaryl substituted pyrazole derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.
CN1915993A Indole group alkaloid of Hainan Gouyahua, and application for preparing drug-breaking medicine This invention discloses chemical structures and extraction method of indole alkaloids including 3-(2-oxopropyl) ibogamine (EHA05) and 3-(2-oxopropyl) ibogamine hydroxyindolenine (EHA06) from Ervatamia hainanensis Tsiang. This invention also discloses the application of the indole alkaloids and their salts for manufacturing analgsics, drugs or food for treating opioid dependence.
CN102366419A Application of rutin and derivative thereof in preparation of antihypoxic medicaments The invention provides a new application of rutin and derivative troxerutin thereof, namely application of preparation of antihypoxic medicaments. An anoxic test of animals and cells proves that rutin and troxerutin have obvious antihypoxic action; the effect has the trend to be better than the effect of nephramid; the antihypoxic medicaments prepared from the rutin and the troxerutin as active components are used for preventing and treating anoxic injury or treating various anoxic pathological states caused by reduced oxygen content in an outside environment and can also be used for preventing or treating anoxic pathological states of heart, brain, respiratory system and the like because normal outside oxygen content cannot thoroughly reach bodies due to diseases; and the antihypoxic medicaments can also be used for preventing or treating the pathological state of insufficient relative supply of oxygen because oxygen consumption required for organic activities exceeds physiological mobilization capability.
WO2006119154A1 Use of pyrimidylamimobenzamide derivatives for the treatment of systematic mastocytosis The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of systemic mastocytosis.
EP1559716B1 Pyrazolonaphthyridine derivative A PDE IV inhibitor which is excellent in antiasthatic effect and the effect of prevention of or treatments for COPD and is highly safe. A compound represented by the general formula (1): (1) (wherein A is a phenyl, pyridyl, 1-oxypyridyl, or thienyl group optionally substituted by one or more substituents selected from the group consisting of hydroxy, halogeno, cyano, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyloxy, amino, carboxy, lower alkoxycarbonyl, carboxy(lower alkylene), (lower alkoxy)carbonyl(lower alkylene), lower alkylsulfonyl, lower alkylsulfonylamino, and ureido; R1 is hydrogen or a substituent selected from the group consisting of hydroxy, halogeno, cyano, nitro, lower alkoxy, amino, carboxy, and lower alkoxycarbonyl; R2 is hydrogen or lower alkyl; and m is an integer of 1 to 3) or a pharmaceutically acceptable salt of the compound has excellent PDE IV inhibitory activity and is highly safe. They are useful as an antasthmatic and preventive/therapeutic agent for COPD.
WO2008132162A1 3- (sulphonylamino) -phenyl-2 -hydroxy-ethylamino derivatives useful as beta-agonists, processes for preparing them and their use as medicaments The present invention relates to compounds of general formula (I), wherein the groups A, L, R1 and R2 have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers, mixtures thereof, solvates thereof, hydrates thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and their use as medicaments.
EP1937656A1 7-(2-amino-1-hydroxy-ethyl)-4-hydroxybenzothiazol-2(3h)-one-derivatives as beta 2 adrenoceptor agonists The present invention provides compounds of formula (I) wherein the variables are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
CN103156872A Adriamycin compound and preparation method thereof The invention provides an adriamycin compound. The adriamycin compound is formed by composition of the adriamycin and a polymer with a structure of a formula (I). The invention further provides a preparation method of the adriamycin compound. The adriamycin compound is obtained through the composition of the adriamycin and the polymer with the structure of the formula (I) in water-based media and the adriamycin and the polymer with the structure of the formula (I) generate an electrostatic interaction. According to the adriamycin compound, the adriamycin is synchronically protected by a hydrophilic polyethylene glycol chain segment and a hydrophobic amino acid chain segment so that sudden release of the adriamycin caused by an influence of a blood circulation system after intravenous injection is effectively avoided and stability of the adriamycin compound is improved. Meanwhile, the prepared adriamycin compound is good in biocompatibility and biodegradability. In addition, carboxyl of the polymer with the structure of the formula (I) and carboxyl of the adriamycin are combined through the electrostatic interaction. The carboxyl has potential of hydrogen (pH) value sensibility in the water-based media so that the release of the adriamycin is accelerated and curative effect of a drug is improved.
WO2012148887A2 Acute cognitive and mood effects of plant polysaccharides in adult human subjects Compositions and methods to improve cognitive performance and mood in an adult human subject's are presented herein. The method of the present invention involved the administration of a dietary supplement comprising plant polysaccharides. The compositions disclosed herein have beneficial effects on memory performance and tasks of high cognitive demand independent of blood glucose responses and despite mental fatigue.
WO2014141118A1 Imidazo[4,5-c]quinoline derivatives and uses thereof The present invention relates to substituted imidazo[4,5-c]quinoline derivatives represented by the compounds formula (I), processes for their preparation, pharmaceutical compositions comprising said compounds and their use in the treatment of diseases or disorders mediated by one or more kinases (such as PI3 kinase, mTOR and ALK-1), particularly proliferative diseases or disorders such as cancer. The compounds of formula (I) can also be used in the treatment of inflammation, angiogenesis related disorders and bacterial infections.
WO2007022734A1 A composition for alleviating a hangover comprising hyaluronic acid and activated carbon A composition for alleviating a hangover comprising hyaluronic acid (HA) and activated carbon , and the use of the combination of hyaluronic acid and activated carbon in the manufacture of products for decreasing the absorption of alcohol and/or preventing the toxicity and injury caused by alcohol , and preventing fatty liver , gastric ulcer , gastrorrhagia and so on caused by excess drinking .
US7048933 Mixing shoots of Pinaceae plants with water and saccharides followed by spontaneous fermenting with yeasts to form remedies for allergic diseases; side effect reduction; for treatment of asthma, atopic dermatitis Remedies for allergic diseases obtained by mixing shoots of plants belonging to the family Pinaceae with water and saccharides followed by spontaneous fermentation. As the plants belonging to the family Pinaceae, is preferable to use plants belonging to the genus Pinus. These remedies, which enable complete recovery in a short administration time without showing any side effects, are useful as remedies for allergic diseases, in particular, asthma and atopic dermatitis. Also, a yeast isolated from these remedies for allergic diseases is provided.
CN1869042A Antisensedigonucleotide structure with withor inhibiting factor survivin gene as target and its use An antisense oligonucleotide is designed and prepared according to the tumor associated wither suppressing factor survivin gene. The 15 antisense oligonucleotides prepared from the bare mouse model of human liver cell cancer are screened and evaluated, which shows that is can suppress the growth of human liver cancer cells and block its gene expression.
US6932988 Comprises brewing black pekoe tea, then adding aspirin tablets, apple cider vinegar, and honey A kit and method for treating migraine headaches comprising the preparing of an oral composition containing at least two bags of black pekoe tea brewed in approximately three ounces of boiling water for ten to thirty seconds. After brewing, the bags of tea are removed and two 325 mg aspirin tablets, one to two teaspoonfuls or tablets of apple cider vinegar, and one to three teaspoonfuls of honey are mixed into the brewed tea. The entire hot and concentrated composition is then cooled over ice so that a person suffering from a migraine headache may quickly drink it.
CN102145058A Medicine preparation for preventing and treating asthenia cold for cattle The invention belongs to the field of veterinary medicines, and provides a medicine preparation for preventing and treating asthenia cold for cattle, which is prepared from the following components in parts by weight: rhubarb, gypsum, sodium bicarbonate, terramycin, dried yeast and so on. The medicine preparation has the effects of relieving diarrhea with astringents, resisting bacteria and relieving swelling, promoting appetite, promoting digestion, strengthening bones, and enhancing immunity, and can not only effectively prevent asthenia cold for cattle, but also can more effectively treat asthenia cold for cattle. Through trail in hundreds of cases, the prevention total effective rate is 90%, the treatment total effective rate is 90%, and the cure rate is 85%. The medicine preparation has a distinct effect and advantages.
CA2157856C Fluoroalkyl/alkenyl-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them There are described benzoylguanidines of the formula I (See formula I) having the definitions of R(l) to R(4) indicated in the text, and their pharmaceutically tolerable salts. They are obtained by reaction of a compound II (See formula II) with guanidine. They are outstanding agents for the treatment of disorders of the cardiovascular system.
EP2150546B1 Pyrimidine derivatives as inhibitors of phosphatidylinositol-3-kinase The invention provides compounds which are pyrimidines for formula (i): wherein R1, R2 are as described herein, and/or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising form abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
WO2012131501A1 Substituted benzimidazole compounds as cot kinase inhibitors Substituted benzimidazole compounds or pharmaceutically acceptable salts thereof are provided, which are useful for treating or preventing diseases, conditions and/or disorders such as asthma, osteoarthritis, rheumatoid arthritis, pain and neurodegenerative diseases by inhibiting Cancer Osaka Thyroid kinase.
WO2012066330A1 Compounds useful as a2a receptor inhibitors According to the invention there is provided a compound of formula I for use in the treatment of a condition or disorder ameliorated by the inhibition of the A2a receptor, wherein the compound of formula I has the structure, wherein, X, A1, A2, R1 and B1 to B5 have meanings given in the description.
CN103735491A Clindamycin phosphate vaginal expansive suppository as well as preparation method and detection method thereof The invention relates to a clindamycin phosphate vaginal expansive suppository as well as a preparation method and a detection method thereof. The expansive suppository consists of a medicated substrate consisting of clindamycin phosphate and a substrate as well as an expansion carrier, wherein the medicated substrate is added with xylitol, dodecyl gallate and triglycerin octyl caprate. The prepared expansive suppository has the effects of high stability, uniform dispersion and the like; meanwhile, the expansive suppository, which is coated with a film coating outside, overcomes hygroscopicity of clindamycin phosphate, and is rapid in drug release and rapid to become effective in the vagina; the disclosed clindamycin phosphate vaginal expansive suppository, through six unique leading technologies, has the beneficial effects of being capable of preventing medicine liquid leakage, avoiding secondary infection and the like.
CA2586553A1 Nasal sprayer containing a formulation with olopatadine A method of delivering a nasal spay. A sprayer having a formulation comprising olopatadine is provided. A spray of the formulation is delivered to a subject~s nose. The spray may have a spray characteristic comprising a spray pattern having a longest axis of 20-45 mm, a shortest axis of 14-20 mm, and an ellipticity of 1-1.8. The spray may also have a spray characteristic comprising a droplet size distribution having a D10 OF 15-30 µm, a D50 of 30-60 µm, a D90 of 50-150 µm, a SPAN of not more than 3, and % Volume of <10 µm of less than 4%.
CN1931170A Gatifloxacin ear drop and its prepn process The gatifloxacin ear drop is prepared with gatifloxacin or its salt as the main component and the supplementary materials including glycerin, ethanol and sterilized water for injection, pure water or distilled water. The present invention also discloses the preparation process of the gatifloxacin ear drop. As one fourth generation oxyquinolone type antibacterial medicine, the gatifloxacin ear drop has high bioavailability, reduced medicine taking times, less systemic untoward reaction, high patient's compliance and less drug resistance.
US20100159000 Medicine for treating gastrointestinal disorder including fecal incontinence A method and a medicine for treating a human having a gastrointestinal disorder that includes fecal incontinence and/or urgency are provided. The method includes administering a dose of the medicine to the human. The medicine includes capsaicin (including one or more of: capsaicin, dihydrocapsaicin, nordihydrocapsaicin, homodihydrocapsaicin and homocapsaicin), a salt of imipramine and ducosate sodium.
EP0772437B9 Compositions for delivery of genetic material Methods of introducing genetic material into cells of an individual and compositions and kits for practicing the same are disclosed. The methods comprise the steps of contacting cells of an individual with a genetic vaccine facilitator and administering to the cells a nucleic acid molecule that is free of retroviral particles. The nucleic acid molecule comprises a nucleotide sequence that encodes a protein that comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen or an antigen associated with a hyperproliferative or autoimmune disease, a protein otherwise missing from the individual due to a missing, non-functional or partially functioning gene, or a protein that produces a therapeutic effect on an individual. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed. Pharmaceutical compositions and kits for practicing methods of the present invention are disclosed.
US20130004559 Flat self-curling permeable sheet membrane A flat self-curling permeable sheet membrane containing a matrix formed of crosslinked biopolymeric fibers. The matrix self-curls into a predetermined shape upon absorption of an aqueous fluid and is permeable to molecules having molecular weights not greater than 1×106 daltons. Also disclosed is a method of preparing such a flat self-curling permeable membrane.
US20060166952 Cardenolide glycosides, which have a cytotoxic activity, cancer 2″oxo-voruscharin compound and derivatives thereof are disclosed as well as pharmaceutical compositions which include 2″oxo-voruscharin compound or derivatives thereof. The disclosed 2″oxo-voruscharin compound and its derivatives are useful for cancer treatment. Methods of treating cancer using the disclosed compounds are also disclosed.
WO2014075146A1 Macrocyclic compounds and uses thereof The present invention relates to novel macrocyclic compounds of Formula I and their use as novel therapeutic agents for example as novel compounds used in methods of preventing and/or treating a disease, condition or state in a subject associated with dysregulation of protease activity and/or dysregulation of proteosome activity
CN101560209B Oxazolidinone compound containing pyridine and preparation method thereof The invention provides an oxazolidinone compound containing pyridine shown in the formula I, a preparation method thereof, and an application of the compound in preparation of medicaments for treatingmicrobe-infected diseases.
EP2266960A2 Aryl-substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles as anticonvulsants Aryl Substituted Pyrazoles, Imidazoles, Oxazoles, Thiazoles and Pyrroles, and the Use Thereof This invention relates to compounds having formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is directed to the use of compounds of formula (I) for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
WO2006054773A1 Activation of caspase in the cell division stage of cancer cells and utilization of caspase inhibitor in anticancer agent and so on It is newly found out that caspase is activated in the cell division stage of cancer cells. By administering a caspase inhibitor, the progress of cell division is retarded in cancer cells and normal chromosome partition is inhibited in the division stage. Moreover, it is observed that the administration of a caspase inhibitor brings about an effect of inhibiting the proliferation of liver cancer origin-cells, cervical cancer-origin cells, etc. An anticancer agent, which comprises as the active ingredient a caspase inhibitor having the effect of inhibiting cancer cell proliferation as described above, is usable an agent against solid cancer such as liver cancer and cervical cancer.
EP1613329A1 Use of 10-hydroxy-10,11-dihydrocarbamazepine derivatives for the treatment of affective disorders The present invention relates to a method for the treatment, including the maintenance treatment, of affective disorders, which comprises administering, especially every 20 to 28 hours, to said subject a therapeutically effective amount, especially an amount between about 500 and about 3000 mg, of a compound of formula (I) wherein R1 represents hydrogen or C1-C3alkyl carbonyl; to the use of a compound of (I) or a pharmaceutically acceptable salt thereof for the manufacture of a pharmaceutical composition for the treatment of affective disorders; to a combination comprising: (a) a compound of formula (I); and (b) at least one compound selected from the group consisting of lithium, divalproex, conventional antipsychotics, atypical antipsychotics, lamotrigine and antidepressants; and to the use of such combination for the treatment of affective disorders.
CN1795851A Application of compound of esters of piperic acid in preparing hypolipidemic or health products An application of peperate compounds in preparing the medicines or health-care food for preventing and treating cardiovascular disease, cerebrovascular disease, hyperlipemia, etc is disclosed.
WO2011140305A2 Method of producing pleurodesis The present invention provides methods of producing pleurodesis in a mammalian subject, comprising administration of a low dosage of a sclerosing agent such as silver or a salt of silver.
CN101559069A Application of 5' nucleotide in preparation of medicines and health-care foods for alleviating physical fatigue The invention relates to an application of 5' nucleotide in preparation of medicines and health-care foods for alleviating physical fatigue. The nucleotide is 5' nucleotide mixture which takes ribonucleic acid (RNA) as raw material, produced by enzymic degradation, has the purity of more than 99%, and is prepared by mixing 5' AMP, 5' CMP, 5' GMPNa2 and 5' UMPNa2 according to the mixture ratio of 22.8:26.6:30.2:20.4. The nucleotide can reduce and prolong the mouse burden swimming time, decreases the generation of blood lactate after movement, lowers the serum urea nitrogen level and has the function of alleviating physical fatigue.
WO2011142316A1 Nitrogen-containing heterocyclic compound having kynurenine production inhibitory activity Disclosed is a nitrogen-containing heterocyclic compound represented by formula (I) or a pharmacologically acceptable salt thereof, which has kynurenine production inhibitory activity. (In formula (I), R6 and R7 may be the same or different and each represents a hydrogen atom or the like; R8, R9, R10 and R11 may be the same or different and each represents a hydrogen atom or the like; R1 represents a lower alkyl group which may be substituted by a cycloalkyl group, or the like; and R3 represents an optionally substituted aryl group or an optionally substituted heterocyclic group.)
CN101766548A Combination of monosaccharides with solar filters and cosmetic use thereof The invention relates to combination of monosaccharides with solar filters and cosmetic use thereof. The present invention relates to a composition, especially a cosmetic and/or dermatological composition, containing, in a physiologically acceptable medium, a combination of at least one monosaccharide chosen from mannose, rhamnose and a mixture thereof, and of at least one sunscreen. The present invention also relates to the use of such a composition.
US20110112123 Compositions for Intratumoral Administration The present disclosure describes compositions for intratumoral administration which include a tissue-stabilizing agent and a therapeutic agent.
CN102526771A Invisible nano-liposome injection for encapsulating USPIO (Ultra-small Super Paramagnetic Iron Oxide) and preparation method and application thereof The invention relates to the technical field of medicine. At present, a USPIO (Ultra-small Super Paramagnetic Iron Oxide) preparation which has high in-vivo target tissue selectivity, high target tissue distribution concentration and high MR (Magnetic Resonance) imaging sensitivity is not reported. A stable and effective invisible nano-liposome preparation is prepared by taking an invisible nano-liposome as a vector, combining MR diagnosis with treatment and carrying USPIO and an anti-tumor medicament simultaneously. Due to the adoption of the invisible nano-liposome injection preparation serving as an MR contrast agent, the in-vivo tissue selectivity of the USPIO can be increased, the sensitivity is increased, and early diagnosis of diseases is facilitated; meanwhile, the invisible nano-liposome injection preparation is taken as a means for evaluating the curative effect of tumor therapy, so that the curative effect of tumor chemotherapy is monitored in real time, overtreatment of a patient is reduced, toxic and side effects are reduced, and the curative effect of tumor chemotherapy is improved.
US20080207549 An antisense polynucleotide or short interfering RNA; diagnosis of proliferative diseases; targets for drug design; antiproliferative agents The present application provides novel human genes WDRPUH and KRZFPUH and PPIL1 whose expression is markedly elevated in a great majority of HCC's and colorectal cancers, respectively, compared to corresponding non-cancerous tissues, as well as novel human gene APCDD1 whose expression is elevated in primary colon cancers and down-regulated in response to the transduction of wild-type APC1 into colon cancer cells. The genes and polypeptides encoded by the genes can be used, for example, in the diagnosis of a cell proliferative disease, and as target for developing drugs against the disease.
EP1562588A2 Use of pde4 inhibitors as adjunct therapy for psychiatric disorders The use of a PDE4 inhibitor in conjunction with psychotherapy provides enhanced therapeutic results in the treatment of psychiatric disorders including, for example, specific phobias, panic disorders, anxiety disorders including posttraumatic stress disorders, and obsessive-compulsive disorder.
US20110251207 Biaryl-spiroaminooxazoline analogues as alpha 2c adrenergic receptor modulators In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
WO2007145922A3 Benzazepinones as sodium channel blockers Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.
US20120129927 New Anthraquinone Derivatives The invention relates to two novel substances, namely (1R,2S,3S,4R)-3-acetoxy-1,2,4,5-tetrahydroxy-7-methoxy-2-methyl-1,2,3,4-tetrahydroanthracene-9,10-dione (3-O-acetyl altersolanol M) and 8-(4,5,6-trihydroxy-7-methyl-2-methoxy-9,10-dioxo-9H,10H-anthracen-1-yl)-(1S,2S,3R,4S)-1,2,3,4,5-pentahydroxy-7-methoxy-2-methyl-1,2,3,4-tetrahydro-9H,10H-anthracene-9,10-dione (the atropisomers alterporriol I and J) to their use as anti-infectives and as anti-cancer agents, as well as to methods of producing the same.
EP1526843A1 Method of preparing solid dosage forms coated in two layers comprising a water-insoluble polymer and a water-soluble pore former A method of preparing a coated solid dosage form is disclosed wherein a solid dosage form, such as a compressed tablet with active agent dispersed therein, is coated at least twice with a coating solution comprising a water-insoluble coating polymer and a water-soluble pore former, and cured after at least the first coating step. The method of the present invention allows for the production of cured coated solid dosage forms using very short curing times. Coated solid dosage forms produced according to the present invention have been found to have long extended release characteristics.
US7358273 For therapy of inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-γ inducing factor-(IGIF), or interferon-γ-(“IFN-γ”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-γ production and methods for treating interleukin-1, apoptosis-, and interferon-γ-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
CN101036710B Oral preparation for treating chough and its preparing process The invention discloses an oral preparation for treating cough and a preparing method thereof, which belongs to medicine technology art. The oral preparation is formed by ephedra herb, poppy shell, glycyrrhiza uralensis, bitter almond, radish seed, ballonflower, gypsum and proper accessory. The key point of the invention is how to select the proper accessory, and how to form a drug having a fine reliable and good curative effect, together with the raw materials. In the invention, by a series of tests, either microcrystalline cellulose or calcium carbonate is selected as an accessory so that flexibility for selecting accessory in the production process is improved. The preparation for treating cough added with the accessory is up to the standard in fluidity of the drug, appearance, moisture, disintegration, etc of the product, thereby, defect in existing technology is conquered, the reliability of the drug is increased.
CN101099742A Testosterone gel preparation capable of decreasing skin irritation The present invention discloses a testosterone gel preparation. It is formed from testosterone, thickening agent, penetrating agent, solvent, pH regulating agent and water.
EP2097389B1 Sulfated benzimidazolone derivatives having mixed serotonine receptor affinity The present invention pertains to compounds of general formula (I) wherein R1, R2, R3, and R4 denote hydrogen or sulfate monoester with the proviso that R1, R2, R3, and R4 cannot simultaneously represent hydrogen, processes for their preparation and their use as pharmaceuticals.
CN1733767A Cyclohexanone analog saturated triring(bridge)compound and its preparation method and uses The invention relates to cyclohexanones saturated tricyclic (bridged ring) compounds containing a long-chain hydrocarbon substituent represented by formula I, extracts containing the compounds, the preparation process and use of the compound and extracts (wherein R1, R2 are defined in the specification). The cyclohexanones saturated tricyclic (bridged ring) compounds provided by the invention can be used as cell cycle inhibitor, cell apoptosis inducer, cell proliferation inhibitor and antineoplastic medicament for anti-tumor treatment.
US20080146585 Use Of C-Kit Inhibitors For Treating Inflammatory Muscle Disorders Including Myositis And Muscular Dystrophy The present invention relates to a method for treating inflammatory muscle disorders including myositis and muscular dystrophy comprising administering a compound capable of depleting mast cells or a compound inhibiting mast cell degranulation, to a human in need of such treatment. Such compounds can be chosen from c-kit inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.
CN103432089A Metformin hydrochloride chewable tablet and preparation method thereof The invention belongs to the field of medical technology and relates to a metformin hydrochloride chewable tablet and a preparation method thereof. The metformin hydrochloride chewable tablet is used for patients suffering from type-2 diabetes with pure unsatisfied diet control, in particular used for patients suffering from obesity and hyperinsulinemia, not only has the effect of reducing blood sugar level but also reducing body weight and alleviating hyperinsulinemia. The metformin hydrochloride chewable tablet is effective for some patients who are treated by sulfonylurea with poor curative effects, and has better effects in combination with sulfonylurea and small intestine glycosidase inhibitors or thiazolidinedione hypoglycemic drugs compared with single use. The metformin hydrochloride chewable tablet can be also used for patients with insulin treatment so as to reduce insulin dosage. The metformin hydrochloride chewable tablet is good in taste, simple and convenient in preparation process and easy to operate, especially suitable for children patients and fills up the blank of medication of children suffering from diabetes.
CN101429191A Uses of substituted tetrahydrochysene isoquinoline derivant The invention relates to a general formula (I) compound and application of salt thereof to preparation of drugs, in particular to application of the salt thereof to preparation of antidiabetic drugs. Pharmacological experiments show that the compound has good antidiabetic effect.
CN102727906A Clathrates of N-methyl-4-(4-(3-trifluoromethyl)benzoylamino)phenoxyl)nicotinamide and salt thereof, preparation method thereof, and application thereof The invention belongs to the field of medicine, and specifically relates to clathrates of N-methyl-4-(4-(3-trifluoromethyl)benzoylamino)phenoxyl)nicotinamide and a 4-methylbenzenesulfonate salt thereof, pharmaceutical compositions thereof, a preparation method thereof, and applications thereof. According to the invention, different preparation means are explored for resolving the technical problems of low solubility and low bioavailability of SKLB 610 and SKLB 710. As a result, the bioavailability or the water-solubility of SKLB 610 and SKLB 710 can be effectively improved by the following steps: adopting SKLB 610 and SKLB 710 as an active component; and adding a carrier material such as beta-cyclodextrin (beta-CYD), hydroxypropyl-beta-cyclodextrin (HP-beta-CYD), sulfobutyl ether-beta-cyclodextrin (SBE-beta-CYD), a mixture of two selected from the above, or a mixture of the three is added to the active component, such that a clathrate is prepared.
CN102579509A Selenium-enriched marasmius androsaceus toadstool extract preparation and preparation method thereof The invention discloses a selenium-enriched marasmius androsaceus toadstool extract preparation which is prepared by the steps that: based on marasmius androsaceus toadstool as a carrier for enriching selenium element, a liquid submerged fermentation technology is adopted, 10-30mg/ml of sodium selenite (Na2SeO3.5H2O) is added into mycelium and metabolite of the marasmius androsaceus toadstool in the growth process according to the volume weight ratio, so that the selenium content in the cultured product of the marasmius androsaceus toadstool reaches 240-400mu g/g; and an excipient is added according to the conventional technology, so that the selenium-enriched marasmius androsaceus toadstool extract preparation is prepared. The selenium-enriched marasmius androsaceus toadstool extract preparation can be used as a medicine for treating multiple pain diseases such as nervous headache, pain in waist and lower extremities, sciatica and the like, and is remarkable in treatment effect; compared with the similar medicines, the selenium-enriched marasmius androsaceus toadstool extract preparation has the characteristics of being high in cure rate, free from side effect or addiction and the like; and the selenium-enriched marasmius androsaceus toadstool extract preparation is simple in production technique, convenient in operation and remarkable in selenium enrichment effect, and has potential application and development values.
WO2010130665A1 Azacyclic spiroderivatives as hsl inhibitors Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein n, m, A, R1 and R2 have the significance given in claim 1. The compounds are useful as HSL inhibitors for the treatment of diabetes dyslipidemia, atherosclerosis and obesity.
CN1768757A Application of a kind of alpha glycosidase inhibitor in preparation of medicine to treat hyperlipemia of diabetes The invention discloses the use of Weilibotang in preparing medicament for the treatment of hyperlipemia of diabetes patients, wherein Weilibotang can improve the symptoms of hyperlipemia for diabetes patients, lower blood triglyceride and cholestrin level, and reduce heart index number.
CN101411738A Novel operation antiblocking liquor The invention relates to a novel surgical anti-adhering liquid capable of effectively avoiding postoperative tissue adhesion. The novel surgical anti-adhering liquid adopts the technical proposal that the novel surgical anti-adhering liquid is characterized by consisting of soybean oil for injection and azithromycin. The novel surgical anti-adhering liquid has lubricating effect and can increase the ability of relative displacement between tissues; a layer of liquid membrane can be formed between the tissues, and has the function of isolating the tissues; because the liquid membrane is formed between the tissues and oppresses the blood capillary, tissue exudation on the wounded surface is inhibited and reduced, wound can be quickly healed; and the azithromycin has strong anti-inflammation, and can inhibit and reduce inflammatory exudation on the wounded surface, thereby facilitating wound healing.
US20110038793 Microsphere comprising an organic lanthanide metal complex The invention provides a microsphere comprising an organic lanthanide metal complex wherein the lanthanide metal is present in an amount of more than 20 wt %, based on total microsphere. The invention further provides a suspension comprising such a microsphere. In addition, the invention relates to a method for preparing said microsphere, and the use of the microsphere(s) or suspension for treating a malignancy and/or obtaining a scanning image.
US20100286247 Methods of Protection from Oxidative Stress Alterations in the structure of telomeres lead to modulation in the redox state of the cell. Substances which mimic destabilized telomeres, such as t-oligos, have a protective effect on future exposure of a cell to oxidative stress.
WO2014111954A1 Process for the preparation and purification of apixaban The present invention provides a process for the preparation and purification of apixaban.
US7351735 (3-Amino-6-phenyl-benzofuran-2-yl)-(2,4-dichloro-phenyl)-methanone; antiprolifrative, anticarcinogenic, antitumor agent; lymphomas, sarcomas, and leukemias This invention relates to novel benzofuran and benzothiophene derivatives of the general table formula and their use for the treatment of hyper-proliferative disorders
WO2014091446A1 Pyrimido [4,5-b]quinoline-4,5 (3h,10h)-diones as nonsense mutation suppressors The invention relates to compound of the formula (I); or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
EP2419105A1 Use of transforming growth factor-b receptor inhibitors to suppress ocular scarring A pharmaceutical composition useful in the prevention of subconjunctival scarring that may occur after GFS comprising an effective amount of an ALK-5 inhibitor. Also disclosed is a method of treating disorder or condition of other ocular scarring or fibrosis including corneal haze and PVR that may develop after ocular surgery or injury comprising applying an amount of a pharmaceutical composition including an ALK-5 inhibitor to a post-surgical or injury site.
WO2010025370A2 Preparation of ranolazine Preparation of ranolazine and intermediates thereof, for use in pharmaceutical compositions comprising ranolazine.
CN1895322A Jinganmin effervescent tablets and preparation thereof A 'Jinganmin' effervescent tablet with high curative effect is proportionally prepared from master medicine, acid source, alkali source, adhesive, lubricant, sweetening agent and flavouring.
US20090297591 Compositions And Methods For The Transdermal Delivery Of Pharmaceutical Compounds The present invention is directed to compositions and methods for the transdermal delivery of a pharmaceutically active compound. In some embodiments, the addition of inert pharmaceutical ingredients in place of a portion of adhesive in a transdermal patch formulation increases the rate of skin permeation of a pharmaceutical compound.
US20100056549 Highly soluble pyrimido-dione-quinoline compounds and their use in the treatment of cancer The present invention features pyrimido-dione-quinoline compounds having improved solubility, pharmaceutical compositions of substituted pyrimido-dione-quinoline compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more pyrimido-dione-quinoline compounds of the invention.
US20120009226 Highly pure laquinimod or a pharmaceutically acceptable salt thereof Provided herein is an impurity of laquinimod, N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide (deschloro laquinimod impurity), and process for preparation and isolation thereof. Provided further herein is a highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity.
US6949521 Therapeutic azide compounds Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.
WO2011158058A1 α-CRYSTALLINE FORM OF CARBABENZPYRIDE The present invention relates to a new crystalline form of carbabenzpyride of formula (I) and the process for its preparation.
CN1969853A Use of N-aryl heterocyclics The invention relates to compounds of formula (I) and the novel use of the pharmaceutical compositions containing them in preparing medicaments for repressing tumor metastasis.
CN101463058B Lanoline alkane type triterpenoid sexangulic acid, derivative thereof and preparation and use thereof The invention relates to the medicine technical field, in particular to lanostane triterpenoid compound sexangulic acid extracted and separated from a Chinese mangrove plant Bruguiera sexangula, derivatives, a preparation method and a use thereof. The structural formula of the sexangulic acid and the derivative thereof are shown in the following formula, when R1 and R2 are simultaneously hydrogen, the compound is the sexangulic acid. A plurality of in vitro anti-tumor activity tests prove that the compound and the derivative thereof can obviously inhibit tumor cell activity and are expected to be applied to preparing anti-cancer drugs. The invention can provide a lead compound for developing new medicines for treating various common multiple cancers, and plays an important role in developing and utilizing living marine resources in China.
CN103735686A Fragrant plant compound essential oil for relieving depression and achieving physical and mental pleasure and preparation method thereof The invention provides fragrant plant compound essential oil for relieving depression and achieving physical and mental pleasure and a preparation method thereof. The fragrant plant compound essential oil comprises the following components in percentage by weight: 25-30 percent of Kushui rose essential oil, 20-25 percent of German chamomile essential oil, 15-28 percent of sandalwood essential oil and 22-40 percent of citron essential oil. The invention further relates to a preparation method of the fragrant plant compound essential oil. The essential oil is small in molecular structure, and can permeate into the skin easily. Essential oil molecules can permeate into the body by massaging, so that absorption is accelerated and both the mind and the body are relaxed. Meanwhile, by using the fragrant plant compound essential oil, the circulation of blood can be invigorated, the lymphatic circulation is promoted, the happiness and protection satisfaction are increased in skin contact, and the physical and psychological health is facilitated. All active components in the fragrant plant compound essential oil come from natural fragrant plants, so that the fragrant plant compound essential oil has the characteristics of mildness and freeness from side effects, can contribute to warming the mood and regulating the feeling, and has the effects of relieving depression and achieving physical and mental pleasure.
CN102885793A Nifuratel compound tablet and preparation method thereof The invention belongs to the field of medical preparations and discloses a nifuratel compound tablet and a preparation method thereof. The nifuratel compound tablet disclosed by the invention has the following advantages of high disintegration speed and dissolving rate, excellent stability, exact dosage, convenience to take and carry, easily-obtained raw materials and low cost. The preparation method of the nifuratel compound tablet is simple in operation, easy to control, time-saving, labor-saving and beneficial for large-scale industrial production.
US20100202979 Compositions and methods for treatment of pulmonary diseases and conditions The invention provides compositions and methods for treating pulmonary diseases and conditions. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists having a binding affinity of 300 fold or greater for α-2 over α-1 adrenergic receptors. The compositions preferably comprise brimonidine and/or dexmedetomidine.
WO2008090631A1 Fucoidan-derived oligosaccharide It is intended to provide a fucoidan-derived low molecular compound with a specified structure and function in which problems regarding absorption property, antigenicity, homogeneity, anti-coagulant activity and the like of fucoidan, which occur when fucoidan being a sulfated polysaccharide with an extremely high molecular weight is developed as a pharmaceutical or a health food, are solved and which has a good taste. By analyzing low molecular compounds obtained by the acid hydrolysis of fucoidan, fucoidan oligosaccharides (I) to (XII) were identified. Further, it was found that the oligosaccharides have an action of preventing obesity or suppressing blood glucose elevation by inhibiting the absorption of carbohydrate or lipid by inhibiting α-glycosidase or lipase.
CN101721508A Oral liquid with functions of strengthening stomach and promoting digestion and preparation method thereof The invention relates to a beverage, and in particular to an oral liquid which has functions of strengthening the stomach and promoting the digestion and is suitable for various groups of people to drink, and a preparation method thereof. The oral liquid comprises chicken's gizzard-membrane, hawthorn fruit, xylo-oligosaccharide, honey, vitamin C, glucose syrup, potassium sorbate and water of which the weight part ratio is 5-15:5-15:1-8:3-9:20-40:0.010-0.02:30-60. The oral liquid with the functions of strengthening the stomach and promoting the digestion has bright color, suitable sour and sweet mouthfeel and rich nutrition, and not only comprises the nutritional components of the hawthorn fruit, the chicken's gizzard-membrane and bioactive substances, but also is added with the vitamin C, the xylo-oligosaccharide, the honey and the like. The product can relieve dyspepsia, remove food retention and strengthen gastric motility function, and has better auxiliary therapy effect on multiple kinds of indigestion, inappetence, gastrectasia and stomachache.
CN102796077A Compound with diuretic effect The invention relates to a compound with a diuretic effect, as well as a preparation method and application thereof, in particular to a compound with the diuretic effect shown as the following formula I in the specifications, pharmaceutically acceptable salt of the compound, a preparation method of the compound and the pharmaceutically acceptable salt, and application of the compound and the pharmaceutically acceptable salt to prevention and treatment of diseases associated with an arginine vasopressin V1a receptor, an arginine vasopressin V1b receptor, an arginine vasopressin V2 receptor, a sympathetic nervous system or a rennin-angiotensin-aldosterone system.
CN101085774A Pidodela prepared from delavirdine intermediate and pidotimod, and synthetic method The invention relates to a kind of pidodela produced with delavirdine intermediate and pidotimod and the synthesizing method, belonging to chemical medical production field. The method is to synthesize pidotimod with delavirdine intermediate and pidotimod through amido bond connection. It is characterized in that the pidodela possesses the combined function of preventing HIV-1 reverse transcriptase of delavirdine and anti-biotic and antiviral because of the ratios of auxiliary T cell and inhibitive T cell are increased or recovered by pidotimod when the immunocompetence is low, it can solve the short half-decay time problem, and the product is expected to be taken orally.
CN102137674A Synthesis and formulations of salts of isophosphoramide mustard and analogs thereof Disclosed herein are formulations and methods of manufacture of compounds of formula (E), wherein X and Y independently represent leaving groups; and A+ is an ammonium cation.
WO2011129549A2 Anticancer drug delivery system using ph-sensitive metal nanoparticles The present invention relates to a method for effectively delivering an anticancer drug into cancer cells by binding the anticancer drug to pH-sensitive metal nanoparticles so as to be separated from cancer cells. The pH-sensitive metal nanoparticles according to the present invention may be heated by photothermal therapy, thereby effectively killing cancer cells in conjunction with the isolated anticancer drug.
CN1861062A Medicine composition used for fish or other aquatic livings and its prepn. method A composite medicine for treating the hemorrhage of aquatic living things (fish, shrimp, crab, turtle, eel, etc) is prepared from benzalkonium bromide, etamsylate, lactic acid and water through proportional mixing.
WO2009032930A3 Compositions comprising human integrin-linked kinase-sirna and methods of use thereof The present invention provides nucleic acid molecules that inhibit ILK expression. Methods of using the nucleic acid molecules are also provided.
WO2009147390A1 Medicaments and methods for inhibition of scarring Provided is the use of an agonist of a GABAA receptor for use in the prevention, reduction or inhibition of scarring formed on healing of a wound. Also provided is a method of preventing, reducing or inhibiting scarring formed on healing of a wound, in which a therapeutically effective amount of an agonist of a GABAA receptor is administered to a patient in need of such prevention, reduction or inhibition. The GABAA receptor agonist used may be an agonist specific to the GABAA receptor, such as Gaboxadol (7-tetra hydroisoxazolo[5, 4-c]pyridin-3-ol), or a pharmaceutically acceptable salt thereof. The scarring to be prevented, reduced or inhibited may be scarring formed on healing of a wound of the dermis.
WO2008113452A1 Substituted tetrahydropyrroloquinolines Compounds of formula (I), in which R1, R2, R3, R4, R5, and R6 and m are defined as cited in claim 1, and can be used to treat tumours and other diseases.
US20070231255 Method for the Treatment of Mammalian Skin Tissues Via Pulse Irradiation in the Presence of a Photoactive Compound A method of treating mammalian skin tissues for causing a predetermined physiological change in the mammalian skin tissues. A treatment composition of matter is applied onto the mammalian skin. The mammalian skin is irradiated with a first pulse having a power density above an activation threshold power density and with a second pulse. The first pulse is emitted for a duration of from about 1 fem-tosecond to about 1 hour, and the first pulse is separated from the second pulse by an inter-pulse interval of from about 1 microsecond to about 10 seconds. The treatment composition of matter includes a photoreactive substance and is applied in an amount sufficient to cause physiological changes within the mammalian skin tissue upon the mammalian skin tissue being irradiated.
EP2618826A1 Phenylpiperidine compounds for the treatment of neurological and psychiatric disorders The present invention relates to a novel use of both enantiomers of the phenylpiperidine derivativ OSU6162, i.e. (-) and (+)-OSU6162 as partial agonists on 5-hydroxytryptamine (5hHT) receptors. As a result, both (-) OSU6162 and (+)-OSU6162 may be used for the treatment and/or prevention of one or more diseases associated with a need for modulation of monoaminergic neurotransmitter receptors, wherein at least one of the monoaminergic neurotransmitter receptors is a 5-hydroxytryptamine receptor (5-HT receptor). Thus, said compounds act as stabilizers not only on dopaminergic, but also on serotonergic brain signaling and will act as partial agonists on such monoaminergic neurotransmitter receptors.
US20080183123 nucleic acid composition for injection; ciliary body tissue(s) or cells and/or to the extra-ocular muscle tissue or cells; antiproliferative, antiinflammatory, antiischemic agent; neurodegenerative diseases; ocular disease, vision deffects The present invention relates, generally, to improved methods of delivering a biologically active agent, in particular a therapeutic or prophylactic nucleic acid, to the ocular sphere of a subject comprising administering said agent to the ciliary body tissue(s) or cells and/or to the extra-ocular muscle tissue or cells. More particularly, the invention relates to devices, their uses, notably in gene therapy, and to methods for treating pathologies of the ocular sphere by specific ciliary body tissue(s) or cells and/or extra-ocular muscle or cells administration of a therapeutic product and transfer thereof into the ocular tissue to be treated. This invention also relates to pharmaceutical compositions comprising the product in a form suitable for ciliary body tissue(s) or cells and/or extra-ocular muscle or cells administration, their preparation and uses.
US20110052740 Skin Circulation-Improving Agent And Skin Temperature-Elevating Agent Skin blood circulation is improved, skin temperature is increased, or shoulder stiffness or sensitivity to cold is prevented or improved by using, as an active ingredient, at least one of the members selected from the group consisting of an Arabian jasmine (matsurika, jasmin sambac) extract, a damask rose (Rosa damascena) steam distillate, 3-methyloctano-4-lactone, and bornyl acetate.
CN103263438A Smokeless moxa cone and preparation method thereof The invention relates to a smokeless moxa cone and a preparation method thereof. The smokeless moxa cone comprises the following ingredients in parts by weight: 90-110 parts of wormwood carbon powder, 3-10 parts of calcium peroxide, and 5-10 parts of hydroxymethyl cellulose. The preparation method comprises the following steps of: evenly mixing the 90-110 parts of wormwood carbon powder, the 3-10 parts of calcium peroxide and 5-10 parts of hydroxymethyl cellulose, then adding 5-10 parts of clear water, and pressing into moxa cones by a machine. In the smokeless moxa cone, the wormwood carbon powder and the calcium peroxide are well mixed and dispersed and adhered as a whole by taking the hydroxymethyl cellulose as an adhesive, and by taking the hydroxymethyl cellulose as a combustion improver, the combustion product is non-toxic and harmless, as well as environment-friendly and pollution-free; in addition, the moxa cone has no smoke, is easy to ignite, fast in combustion speed, high in radiation temperature, and strong in moxibustion force, and the preparation method is simple, low in cost and suitable for popularization.
US20110305670 Nucleic acid encoding fusion polypeptides that prevent or inhibit hiv infection The present invention is directed to an isolated nucleic acid molecule encoding a fusion polypeptide the expression of which in cells is capable of blocking the entry of HIV-1 into host cells and methods of using the nucleic acid molecule.
CA2740135A1 Nitric oxide-releasing dressings The invention relates to the use of nitric-oxide-releasing anti-septic agents in wound dressings. The dressing may comprise a bottom layer that is permeable to gaseous NO and an upper surface barrier that is relatively gas and moisture-impermeable to prevent premature dispersion of the gas. The dressings comprise a plurality of layers, one layer comprising a supply of sodium nitrite and citric acid, and another layer comprising a supply of water contained within capsules and/or frangible packets. Release of NO occurs when sodium nitrite and citric acid come into contact with the water supply. This activation is performed either by applying pressure on the dressing which will result in the breakage of the capsules and/or packets or through a pull-tab attached to such capsules and/or packets. The dressings may further comprise an oxygen-releasing component.
CN102367252A Tropisetron hydrochloride compound Belonging to the field of medical technologies, the invention specifically relates to a tropisetron hydrochloride compound. The invention also relates to application of an injection containing the tropisetron hydrochloride compound in the crystal form of the invention in preparing medicaments for treating nausea and vomiting.
WO2005000806A2 Ligands for nicotinic acetylcholine receptors, and methods of making and using them One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.
US20100286063 GNRH agonist combination drugs In the field of pharmaceuticals, it is intended to provide drugs whereby the preventive and therapeutic effects of a GnRH agonist on various diseases can be enhanced and QOL can be improved. More specifically, combination of drugs characterized in that the GnRH agonist is combined with a chemical selected from among SERM, SARM, sex hormone synthesis inhibitors, receptor-type tyrosine kinase inhibitors, bone metabolism regulators, drugs for immunotherapy, cytokine/chemokine inhibitors and endothelin receptor antagonists. Owing to these combinations, excellent effects of enhancing the preventive and therapeutic effects of the GnRH agonist on various diseases and relieving side effects can be established. Furthermore, QOL can be improved thereby.
CN101073557A Formula of natural beta-carotene sub-micrometer emulsion and its production The invention is concerned with the compounding and technics of beta-carptemes submicron emulsion, which the beta-carptemes preparation can stabilizing with the capability of decentrality, light fastness, oxytolerant, and temperature tolerance in water. The invention can be used in food, beverage, health products, and cosmetic as coloring agent, nutrition tonic and anti-oxidants.
EP1408940B1 Pharmaceutical composition comprising deramciclane for the treatment of the decline and/or damage of cognitive functions The compounds of the general Formula (I) (wherein R stands for hydrogen or methyl) can be used for the treatment or prophylaxis of diseases characterized either by the decline and/or damage of cognitive functions, or mental disability accompanying other diseases. As compound of the general Formula I preferably -(1R,2S,4R)-(-)-2-(2-dimethylaminoethoxy)-2-phenyl-1,7,7-trimethylbicyclo[2.2.1]heptane-fumarate can be used.
CN101318012A Application of beta-inhibited protein 1 in governing survival and autoimmunity of T cell The invention relates to an application of Beta-inhibitory protein 1 in regulation of T cellular survival and autoimmunity, in particular to the use of inhibitor of Beta-inhibitory protein 1 in preparing drugs. The inhibitor of Beta-inhibitory protein 1 is selected from (i) the material inhibiting the activity of Beta-inhibitory protein 1; (ii) the material inhibiting genetic transcription, translation or the both of Beta-inhibitory protein 1, the drug is used for treating or preventing diseases of the objectives of mammal which are related to apoptosis abnormality of the CD4<+>T cellular.
CN101372514A Scaphium scaphigerum polysaccharide, preparation and use thereof The invention discloses a Pangdahai polyoses and a preparation method thereof. The method comprises Pangdahai materials which are degreased and pretreated by ethanol are added with water to be treated by ultrasonication, and then is heated up to 55-65 DEG C to be extracted; after that the extracting solution is concentrated, processed by ethanol precipitation and purified according to the conventional method. By adopting ultrasonication and water bath extraction with lower temperature, the obtained Pangdahai water soluble polyoses has higher yield and purity as well as better anti-inflammation activity.
CN101310767A Cryosurgery anticancer antigen preparation and preparation method thereof The invention discloses an anti-cancer drug preparation, in particular to a cryosurgical antigen preparation and a preparation method thereof. The cryosurgical antigen preparation is characterized in that: the cryosurgical antigen preparation is prepared by raw materials with the following mix ratio: 10g of tumor sample which removes non-tumor tissues, 0.1 to 0.3g of sword jackbean seed extract liquid, 0.8 to 1.2 million units of interleukin-2, 1 to 3g of soybean liposome and 0.1 to 0.3g of lidocaine. CAAP clinically applies the efficacy special detection of skin test, which is initially created by an author, and the method is simple and easy to operate, thus being deeply welcomed by patients and medical staff. Three same principles of the same species, the same organs and the same tumor type are the important theory and material foundation for advocating a tumor bank by the author and implementing the CAAP tumor biological treatment. The strict specificity and the personalized treatment need to be used by using a key to open a lock and not to be confused, thus being the important guarantee for the CAAP radical effect.
CN101411788A Method for preparing powder for whitening teeth The invention discloses a method for preparing re-whitening powder, which comprises the following steps: various medicines are ground into fine powder, are loaded into a bottle, and are sealed. A small amount of the re-whitening powder is used to brush teeth, which can quickly re-whiten various sick teeth, firmly fix the teeth until old age, and ensure that the teeth can keep intact.
CN1939265A Oral preparation containing cefoperazone and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains cefoperazone. Its preparing process is also disclosed.
CN1806796A Pharmaceutical composition containing valibose, its preparation method and application The invention relates to a pharmaceutical composition containing Weilibo sugar and its preparing process, wherein the composition comprises 0.5-50mg of pharmaceutically acceptable Weilibo sugar and optional carrying agent. The invention also provides the use of the pharmaceutical composition in the preparation of medicament for the treatment or prevention of diabetes and diabetes-related diseases.
US7737161 such as 5-amino-N-(5-chloropyridin-2-yl)-3-{[(trans-4-pyrrolidin-1-ylcyclohexyl)carbonyl]amino}furo[3,2-b]pyridine-2-carboxamide, used as activated blood coagulation factor X inhibitors The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.
CN103169733A Compound probiotic, application thereof for treating anaphylactic diseases and allergy free probiotic electuary for pregnant and lying-in women The invention relates to the field of medicines, and in particular to compound probiotic, application thereof for treating anaphylactic diseases and allergy free probiotic electuary for pregnant and lying-in women. The compound probiotic consists of bifidobacterium Bi-07, lactobacillus rhamnosus LR22, lactobacillus acidophilus NCFM. The compound probiotic not only can irritate secretion of IFN-gamma and IL-2 in animal body, but also inhibit secretion of immune globulin E (IgE) and IL-4 so as to prevent and treat anaphylactic diseases. The invention further provides a medical preparation comprising the compound probiotic and allergy free probiotic electuary for pregnant and lying-in women. The pharmacodynamic test shows that the medical preparation has remarkable effect of improving IL-2 and IFN-gamma. In addition, compared with the control group, the content of IgE in the test group is further remarkably reduced. Long-term clinical tests show that the medical preparation comprising the compound probiotic provided by the invention is free from untoward effects to human body.
US8617540 Combinational chemotherapy treatment Disclosed is a composition comprising a therapeutically effective amount of (a) at least one compound from the group of 5-fluorouracil, 5-fluorodeoxyuridine, capecitabine or a prodrug of such compounds; and (b) 5-hydroxymethyl-2′-deoxyuridine, or a prodrug of such compound, as well as kits comprising such composition and methods of use thereof for treating neoplasia.
CA2790240A1 Use of tigecycline for treatment of cancer Cancer stem cells exhibit different metabolic profiles from other cancer cells, such that they do not readily respond to treatment using conventional chemotherapeutic agents. Studies disclosed herein now demonstrate that the glycylcycline antibiotic tigecycline (a tetracycline derivative) exhibits anti-cancer activity, including activity against cancer stem cells. This anti-neoplastic activity appears to be due to inhibition of mitochondrial protein synthesis in the cancer cells. In preferred embodiments, the cancer to be treated is a hematological cancer, such as leukemia, lymphoma or myeloma.
WO2010002472A1 Jak kinase modulating compounds and methods of use thereof Provided herein are pyrrolotriazine compounds for treatment of JAK kinase, including JAK2 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
CN103432087A Clindamycin hydrochloride preparation for injection and preparation method thereof The invention discloses a clindamycin hydrochloride preparation for injection and a preparation method thereof. The preparation is prepared from clindamycin hydrochloride and auxiliary materials such as Fe3O4 magnetic powder and carboxymethyl glucose. In the preparation process, Fe3O4 magnetic powder and carboxymethyl glucose mixed are stable in property to easily form microballoons with certain strength and can be fully encapsulated or the medicine completely enters into a carrier framework, relatively. After injection, the medicine can be reasonably released in human body, so that the pharmacological activity of the medicine is maintained and the bioavailability of the medicine is improved. Meanwhile, the time of deliveries of medicines to be used for a long time can be reduced due to the sustained-release preparation, so that balance of blood concentration can be maintained, the peak valley phenomenon is avoided, and untoward effects of the medicine are reduced. In addition, the iron content of the carrier in the preparation does not affect normal total iron supplementing amount of the patient, and magnetic particles can be safely discharged outside the human body through normal excretion of the human body.
EP2179993A1 Sulfoxide substituted aniline pyrimidine derivatives as CDK inhibitors, their manufacture and use as medicine Phenyl-(5-trifluoromethyl-pyrimidin-2-yl)-amine compounds (I) and their salts, diastereomers or enantiomers are new. Phenyl-(5-trifluoromethyl-pyrimidin-2-yl)-amine compounds of formula (I) and their salts, diastereomers or enantiomers are new. R 1>1-6C-alkyl, 2-6C-alkenyl, 2-6C-alkynyl, 3-7C-cycloalkyl or phenyl ring (all optionally substituted by OH, NR 3>R 4>, CN, halo, CF 3, 1-6C-alkoxy, OCF 3 and/or 1-6C-alkyl); R 2>1-10C-alkyl, 3-10C-alkenyl, 3-10C-alkynyl or 3-7C-cycloalkyl ring (all optionally substituted by halo, OH, NR 3>R 4>, CN, CF 3, OCF 3, 1-6C-alkoxy, 1-6C-alkyl, 2-6C-alkenyl, 2-6C-alkynyl, or 3-8C-cycloalkyl, -O-CH 2-phenyl, C n-alkoxycarbonyl (optionally substituted by halo, OH, 1-6C-alkyl, 1-6C-alkoxy, NR 3>R 4>, CF 3 and/or OCF 3)), preferably alcohol group of formula (A); R1a : CH 3, C 2H 5, propyl or isopropyl; R1b, R1c : H, CH 3 or C 2H 5; either R 3>, R 4>H, 1-6C-alkyl, 2-6C-alkenyl, 3-8C-cycloalkyl, phenyl ring, 3-8 membered heterocycle ring, and/or a monocyclic heteroaryl ring (optionally substituted by OH, NR 5>R 6>, CN, halo, CF 3, 1-6C-alkoxy and/or OCF 3); or R 3>R 4>N : 5-7-membered ring optionally containing 1 or 2 further heteroatoms in addition to N, and optionally substituted by OH, NR 5>R 6>, CN, halo, CF 3, 1-6C-alkoxy and/or OCF 3; and R 5>, R 6>H or 1-6C-alkyl (optionally substituted by OH, CN, halo, CF 3, 1-6C-alkoxy and/or OCF 3). An independent claim is included for the preparation of (I). [Image] [Image] - ACTIVITY : Cytostatic; Virucide; Cardiovascular-Gen.; Vasotropic; Antiarteriosclerotic. - MECHANISM OF ACTION : Cyclin-dependent kinase inhibitor; Vascular endothelial growth factor receptor kinase-2 inhibitor. The ability of (I) to inhibit cyclin-dependent kinase was tested in recombinant cyclin-dependent kinase-1 and B-type cyclin-glutathione-S-transferase-fusion proteins purified from baculovirus infected insects cells. The results showed that (2R,3R)-3-[2-(4-methanesulfonyl-phenylamino)-5-trifluoromethyl-p yrimidin-4-yloxy]-butan-2-ol exhibited an IC 5 0 value of 7 nM.
WO2012067138A1 Novel polymer derivative of cytidine metabolism antagonist [Problem] To provide a novel polymer derivative of a cytidine metabolism antagonist with which drug release is possible independent of a biological enzyme and with which a highly therapeutic effect is expected. [Solution] A polymer derivative of a cytidine metabolism antagonist in which substituent groups represented by general formula (I) or general formula (II) [where R7 and R8 are each independently a hydrogen atom or C1-6 alkyl group optionally having substituent groups; R6 is a hydrogen atom, C1-40 alkyl group optionally having substituent groups, C1-40 aralkyl group optionally having substituent groups, aromatic group optionally having substituent groups, amino acid residue protected by carboxy groups, or sugar residue optionally having substituent groups; CX-CY is CH-CH or C=C (double bond); and A is a residue in which the amino group at position 4 has been removed from the cytidine metabolism antagonist] are bonded to the side chain carboxy groups of a block copolymer formed by a polyethylene glycol structural segment and a polymer having ten or more carboxy groups.
EP2422787A1 Diazoxide for use in the treatment of amyotrophic lateral sclerosis (als) The invention relates to the diazoxide or a pharmaceutically acceptable salt thereof for use as a medicament at low doses to treat amyotrophic lateral sclerosis.
US20090053303 Medical food or nutritional supplement, method of manufacturing same, and method of managing diabetes A medical food and/or nutritional supplement for oral administration by mammals includes α-lipoic acid, linolenic acid complex, biotin, and coenzyme Q-10. A preferred method of manufacturing the medical food or nutritional supplement is by separate microencapsulation of one or more of the components followed by encapsulation of the individual components, for oral administration. Other methods of delivery include packaging in impermeable, disposable packets and mixing the formulations with food or a cold liquid.
WO2007140358A3 Treatment of polyglutamine-expansion neurodegenerative diseases The invention relates to methods for stimulating fast axonal transport in polyglutamine expansion diseases and treating polyglutamine expansion diseases by inhibiting SAPK- dependent phosphorylation of kinesin. The present invention also provides methods for identifying agents which inhibit the phosphorylation of the kinesin, as well as methods for monitoring treatment of a polyglutamine expansion disease based on the phosphorylation of serine 176 of kinesin-1A or kinesin-1C, or serine 175 of kinesin-1B.
CN101185643A Application of (E)-1-(2, 4-dihydroxy-5-(3-methyl-butyl-2-alkenyl) phenyl)-3-(4-hydroxy-phenyl) propylene-2-ketone-1 in medicine The invention relates to a chemical compound (E)-1-(2,4-dihydroxy- 5-(3-methyl-butyl-2-alkenyl) phenyl)-3-(4-hydroxyphenyl)-propylene-2-ketone-1 and the application of the salt and solvate thereof acceptable in pharmacy in preparing drugs used for treating diseases related to estrogen receptor ER-Alpha subtype and ER-Beta subtype, belonging to the field of pharmacology. The chemical compound does not change expressions of ER-Alpha 66, ER-Alpha 46 and ER-Alpha 36 under the low concentration condition, while the expressions can be simultaneously inhibited under high concentration condition; meanwhile, the compound can kill the breast cancer MCF7 cells which can express ER-Alpha 66, ER-Alpha 46 and ER-Alpha 36; therefore, the compound can be used as a moderator of estrogen receptor ER-Alpha 36 for treating diseases such as tumor, osteoporosis, asthma, heart diseases, senile dementia, etc. caused by abnormal expression of estrogen receptor ER-Alpha 36.
US20120141483 Methods of treating or preventing psoriasis, and/or alzheimer's disease using indane acetic acid derivatives The present invention provides indane acetic acids and their derivatives and methods for the treatment and/or prevention of psoriasis and/or Alzheimer's diseases using the same.
CA2464687A1 Spirastrellolides, antimitotic macrolides and analogues; and pharmaceutical compositions and research tools thereof A series of novel antimitotic macrolides based on the structure of Spirastrellolide A, which was isolated from the Caribbean marine sponge Spirastrella occinea, are described. Spirastrellolide A has a 47 carbon linear polyketide backbone incorporated into a highly functionalized 38 membered lactone containing a tetrahydropyran and two spiro bispyran substructures embedded in the macrocycle and a side chain terminating in a carboxylic acid. Spirastrellolide A's structure was elucidated by detailed spectroscopic analysis of its methyl ester. Spirastrellolide A methyl ester shows potent activity in a cell-based assay that detects mitotic arrest, but it does not affect tubulin polymerization in vitro. It has the unusual biological property of being able to accelerate entry of cells into mitosis from other cell-cycle stages, before it arrests them in mitosis.
CN1895584A Freckle-dispelling beverage A health-care spot removing beverage is prepared from 11 Chinese-medicinal materials including honey, glutinous rice, calcium lime, almond, etc through drying, pulverizing and treating with purified water.
WO2008123758A1 Pharmaceutical composition comprising n-sulphoethylnicotinamide useful in treatment or prevention of a pulmonary disease and use of said composition for treatment or prevention of said disease The present invention concerns a compound for treating or preventing a pulmonary disease, the compound having the following formula: N-sulphoethylnicotinamide (NESA, [N-nicotinamide] - ethanesulphonic acid 2) and the pharmaceutically acceptable derivatives thereof. In a preferred embodiment of the invention a pharmaceutical composition comprises the compound N-sulphoethylnicotinamide (NESA) or a pharmaceutically acceptable derivative thereof. The purpose of the composition is to treat or prevent a pulmonary disease. In particular, the composition comprises between approximately 7 mg and approximately 1 g of N-sulphoethylnicotinamide (NESA) or a pharmaceutically acceptable derivative thereof. Preferably, the composition comprises between approximately 140 mg and approximately 800 mg of N-sulphoethylnicotinamide (NESA) or a pharmaceutically acceptable derivative thereof. More preferably, the composition comprises between approximately 250 mg and approximately 500 mg of N-sulphoethylnicotinamide (NESA) or a pharmaceutically acceptable derivative thereof.
EP2700642A1 Camptothecin compound containing stable 7-membered lactone ring, preparation method and use Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1∼C3 alkyl, acetyl or propionyl; R2 is H, a C1∼C6 alkyl, a C3~C6 cycloalkyl, piperidyl; or a C1∼C6 alkyl substituted by an amino; R3 is H, a C1∼C3 alkyl, or a C1∼C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1∼C6 alkoxy; R5 is H, or a C1∼C6 alkoxyl; or R4 and R5 are linked to each other to form -OCH2O- or -OCH2CH2O-. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.
EP1931333A1 Amino acid and its uses This invention relates to a supplement, the use thereof and method for supplementing the concentration of free cellular L-proline in an organism, for restricting dehydration of such an organism, the supplement comprising an effective amount of free L-proline. The supplement is effective in reducing the levels of free radicals in organisms experiencing water stress. This invention further relates to a method of treating dehydration in humans and animals including the step of administering to an individual in need thereof an effective amount of a supplement according to the third aspect of the invention. An effective amount of free L-proline is typically between 20 and 1000 mg, preferably 100 mg free L-proline per kilogram body mass of the organism, three times a day.
WO2011041512A3 Compositions and methods for treating mlv-infection, and preventing and treating mlv-initiated diseases Compositions and methods for inhibiting infection by XMRV or other MLV are disclosed. Also disclosed are methods for treating cancers resulting from infection by XMRV or other MLV, and for preventing such cancers. The anti- XMRV/anti-MLV compounds are predominantly integrase inhibitors, such as globoidnan A, L-000870812, S/GSK1349572, S/GSK1265744, Raltegravir and Elvitegravir, and also reverse transcriptase inhibitors AZT, tenofovir, and tenofovir DF. The compounds are also useful for treating chronic fatigue syndrome or other diseases with neuroimmune symptoms resulting from an infection by XMRV or other MLV. The compositions can also include other therapeutic agents known for treating prostate cancer, breast cancer, lymphomas, and leukemias, such as anti-androgenic agents, radioisotopes, and conventional anti-cancer compounds.
US7754220 Continuously administering to a male animal a polypeptide havingan amino acid sequence to promote the activity of Metastin, (kisspeptin-54), an endogenous ligand for G protein-coupled receptor; promoters of fertility, ovulation; treating hormone-sensitive cancers; endometriosis; drug screening Metastin, compounds that promote the activity of metastin or its receptors and the like are excellent gonadal function improving agents, ovulation inducers or promoters, gonadotropic hormone secretion promoters, gonadotropic hormone secretion inhibitors, sex hormone secretion promoters, sex hormone secretion inhibitors, etc., and can be used as agents for preventing/treating sterility, hormone-sensitive cancers, endometriosis, etc. Metastin and its receptors are useful for screening for these pharmaceuticals.
CN103204781A 2, 7-bi-substituted fluorenone derivative and preparation method and application thereof The invention relates to a 2, 7-bi-substituted fluorenone derivative and a preparation method and application thereof. The structural formula is shown as 2-hydroxy-3-amidopropyl, 2-amido, wherein R refers to halogenated hydrocarbon. The preparation method is simple and high in yield. Most compounds have good in-vitro antitumoral activity.
WO2012061015A2 L-citrulline supplementation during arginine depletion therapy with arginase The present invention concerns methods and compositions for reducing toxicity of an anticancer agent that involve citrulline or an analog thereof. Nonlimiting examples of anticancer agents include arginine depletion agents.
US20130035368 Oligonucleotide compounds comprising non-nucleotide overhangs The invention relates to siRNA compounds comprising one non-nucleotide moiety covalently attached to at least one of the sense or antisense strands to down-regulate the expression of human genes. The invention also relates to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier and to methods of treating and/or preventing the incidence or severity of various diseases or conditions associated with the target genes and/or symptoms associated with such diseases or conditions.
CN101904862A Water-soluble vitamin composition freeze-drying preparation for injection The invention discloses a water-soluble vitamin composition freeze-drying preparation for injection. The freeze-drying preparation comprises the following raw materials and is prepared into 1,000 bottles: 2.8 to 3.4 grams of thiamine mononitrate, 36 to 44 grams of nicotinamide, 4.4 to 5.4 grams of pyridoxine hydrochloride, 14.8 to 18.1 grams of sodium pantothenate, 4.4 to 5.4 grams of riboflavin sodium phosphate, 102 to 124 grams of sodium vitamin C, 54 to 66 milligrams of biotin, 0.36 to 0.44 gram of folic acid, 124.5 to 6.0 milligrams of vitamin B, and 0.4 to 0.6 gram of methyl-p-hydroxy benzoate, wherein the nicotinamide is nicotinamide hydrate, and the sodium pantothenate is sodium pantothenate hydrate. The water-soluble vitamin for injection has adjustable grain size, concentrated grain size distribution, glabrous surface, high product fluidity, greatly improved stability and high dissolution rate, and a preparation process of the preparation is simple and is favorable for popularization and use.
US7040311 Closure-cap and container as a two-chamber cartridge for nebulizers for producing aerosols and active substance formulations, suitable for storage The invention relates to an apparatus comprising a closure-cap and a container in the form of a two-chamber cartridge in which an active ingredient and a solvent can be stored separately until the apparatus is used in a nebulizer, as well as an active substance concentrate in which the active-substance is present as a solution or suspension for storage purposes.
CN102526049A Compound diclofenac sodium slow-release preparation and preparation method thereof The invention discloses a compound diclofenac sodium slow-release preparation and a preparation method of the compound diclofenac sodium slow-release preparation. The compound preparation consists of the following ingredients in percentage by mass: 20 to 30 percent of diclofenac sodium, 4 to 8 percent of omeprazole or sodium salt of the omeprazole and the balance of auxiliary materials allowed on the pharmacy. The preparation method of the compound preparation comprises the steps that: the diclofenac sodium and the omeprazole are respectively prepared into enteric granules or pellets, the prepared omeprazole enteric granules or pellets are mixed with the diclofenac sodium enteric granules or pellets, and the tabletting or the capsule filling is carried out. In compound diclofenac sodium enteric slow-release tablets or enteric slow-release capsules prepared by the preparation method, the medicine release of the main omeprazole medicine is carried out at the normal release speed, but the diclofenac sodium is slowly released from the preparation. Therefore, the omeprazole or the sodium salt of the omeprazole is firstly released for realizing the effect of protecting the gastrointestinal mucosa, the diclofenac sodium is prevented from irritating the gastrointestinal mucosa of a patient in the medicine release process, and the gastrointestinal tract adverse reaction occurrence rate of the diclofenac sodium is reduced.
WO2014028805A1 Pyrrolopyrazoles as n-type calcium channel blockers Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: Formula. (I) wherein R1, R2 R3, Q, and G are defined herein.
US7312221 Therapeutic treatment of endotoxic shock with a 4-[piperazine-1-yl]-1,2-dihydro-quinolines; treating psoriasis, arthritis, osteoarthritis, glomerulonephriti, autoimmune disorder include diabetes, asthma, or multiple sclerosis Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.
US7432308 Therapeutic compositions for the treatment of a respiratory tract disease The equilibrium between G actin and F actin is shifted towards the F actin confirmation with compounds such as the ionic form of magnesium or potassium. The higher amount of F actin decreases the inhibition of nucleases such as DNAse I by monomeric G actin. The increased performance of the nuclease results in better treatment of patients suffering from cystic fibrosis or other diseases with viscous mucus.
US20060177524 Ocular irrigating solution A disclosed ocular irrigating solution for irrigating the eye during surgery comprises a source of bicarbonate ions and a physiologically acceptable organic buffer which is an organic zwitterionic buffer having a buffering capacity with in the range pH 6.8 to 8.0.
CN1886138A CDK2 antagonists as short form C-MAF transcription factor antagonists for treatment of glaucoma The short form version of c-Maf transcription factor is up-regulated in steroid-treated and transforming growth factor beta2-treated trabecular meshwork cells, and is present at elevated levels in glaucomatous versus normal trabecular meshwork cells and in glaucomatous versus normal optic nerve head tissue. Expression of short form c-Maf transcription factor under these conditions indicates a causal or effector role for the factor in primary open-angle and steroid-induced glaucoma pathogenesis. Antagonism of short form c-Maf transcription factor expression and/or activity in the trabecular meshwork or other ocular tissue is provided for inhibiting or alleviating glaucoma pathogenesis. Antagonists include cyclin-dependent kinase 2 inhibitors.
WO2008100635A8 1- [3- (monocyclic amino) propyl] - 4, 5, 6, 7-tetrahydro-1h-pyrazolo [4, 3-c] -pyridines as modulators of cathepsin s Monocyclic aminopropyl tetrahydro-pyrazolo-pyridine compounds of formula (I) are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis. Formula (I), wherein: R1 and R2 taken together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl group; wherein: R1 and R2 taken together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl group, optionally containing one additional heteroatom ring member that is O, S, SO2, or NRa, and being unsubstituted or substituted with one, two, or three Rb substituents; and wherein R3-R8, Ra, Rb and n are as defined herein.
US20080219973 Using antigalectin-3 immunoglobulin as therapeutic in prevention and treatment of glomerulonephritis, diabetic nephropathy and/or tissue fibrosis A pharmaceutical composition having an inhibitory effect on the overproduction and the accumulation of extracellular matrix, said composition comprising as an active ingredient a compound that inhibits the biological activity of galectin-3, which pharmaceutical composition can serve as a therapeutic or preventive agent for glomerular nephritis, diabetic nephropathy or tissue fibrosis, as well as the use of said compound for the production of pharmaceuticals for the above-mentioned use, and a method for inhibition of the overproduction and accumulation of the extracellular matrix.
WO2012020892A1 Rhus verniciflua stokes extract having increased content of active flavonoid compound and method for preparing same The present invention relates to Rhus verniciflua Stokes extract having an increased content of an active flavonoid compound through a gas bubbling treatment, a method for preparing the Rhus verniciflua Stokes extract, and a method for converting fustin into fisetin through the gas bubbling treatment of a solution containing fustin. The method for preparing the Rhus verniciflua Stokes extract of the present invention can convert the conventional Rhus verniciflua Stokes extract having high content of fustin and low content of fisetin into a Rhus verniciflua Stokes extract having high content of fisetin. Therefore, the Rhus verniciflua Stokes extract of the present invention can be commercialized into natural anticancer agents, anticancer and cancer prevention food products, and health functional foods due to the excellent bioactivity thereof, and promote the development of relevant industries through the high added-value of Rhus verniciflua Stokes. In addition, the method for converting fustin into fisetin can be applied to other natural substances and be used as a method for enhancing the functionality thereof by increasing the content of highly active flavonoid, thereby becoming an enabling technology that can lead high-functionalization of natural substances.
DE102009003974A1 Oral high-dose vitamin K1-containing preparation, useful for increasing the resistance of the human organism against influenza infection High-dose vitamin K1-containing pharmaceutical preparation for oral administration, is claimed. - ACTIVITY : Virucide. No biological data given. - MECHANISM OF ACTION : gamma -Carboxy-glutamic acid proteins activator.
CN102051394A Preparation method and application of sulfo-diketopiperazine compounds The invention belongs to the technical field of medicines, and relates to a preparation method and application of sulfo-diketopiperazine compounds. The preparation method provided by the invention comprises the following steps: separating a sea mud sample, which is acquired from the intertidal zone of the Bohai Sea rim area in Yingkou, Liaoning, to obtain fungus Aspergillus fumigatus; and fermenting a large amount of Aspergillus fumigatus, filtering the fermentation liquid, extracting the fermentation liquid with ethyl acetate to obtain an extract containing sulfo-diketopiperazine compounds, and separating and purifying the sulfo-diketopiperazine compounds from the extract. The method provided by the invention is simple and easy to operate, and has the advantage of favorable repetitiveness. The prepared compounds have obvious function of inhibiting the growth of tumor cell strains, and are expected to become lead compounds of antineoplastic medicaments.
US20080089884 For treating and/or preventing bladder disorders; for decreasing the expression, release or biological activity of macrophage migration inhibition factor The invention relates generally to methods for treating and/or preventing bladder disorders. In certain embodiments the invention comprises methods for the treatment and/or prevention of a bladder disorder comprising administering an effective amount of a therapeutic agent that decreases the expression, release or biological activity of macrophage migration inhibition factor (MIF) to a subject in need thereof. In other aspects the invention relates to a method for diagnosing bladder disease and/or bladder disease severity comprising screening for a MIF gene or MIF receptor gene polymorphism or expression level.
WO2005011707A1 A doxycycline metal complex in a solid dosage form The present invention is a solid dosage form of a doxycycline metal complex. The present invention also includes a process for making a doxycycline metal complex in a solid dosage form. The process comprises the steps of (i) providing an aqueous solution of doxycycline or a physiologically acceptable salt thereof; (ii) admixing a metal salt with the aqueous solution; (iii) admixing a base to increase the pH of the aqueous solution, thereby forming a suspension of doxycycline metal; and (iv) drying the suspension, thereby forming a dry granulation of doxycycline metal complex.
EP1610785B1 Pharmaceutical combination for the treatment of spasticity and/or pain The present invention relates to a pharmaceutical combination for the treatment of spasticity and/or pain characterized by that the combination contains as active ingredient 70-95% w/w compound of formula (I), wherein R represents a methyl or ethyl group, and 5-30 % w/w dextromethorphan (chemical name: (+/-)-3-methoxi-17-methylmorphinan).
US20100286196 New inhibitor of dd-peptidase and its use as antibiotic or anticancer drug A new compound is revealed and the strain of Streptomyces sp. producing it, which may be used in the production of drugs (Formula I).
WO2011008298A3 Novel axomadol dosage forms The present invention provides a slow release dosage form comprising a therapeutically effective amount of at least one form of axomadol, at least one pharmaceutically acceptable excipient wherein the said dosage form is suitable for once or twice daily administration. This invention also provides a method of treating a mammal by administering such slow release dosage forms. The present invention also provides a dosage form comprising a therapeutically effective amount of at least one form of axomadol, at least one pharmaceutically acceptable excipient, and at least one second active agent, wherein the second active agent is selected from a group consisting of acetaminophen, an NSADD, an Opioid, an Antiepileptic, a Norepinephrine Reuptake Inhibitor, a Serotonin Norepinephrine reuptake inhibitor (SNRI), a Cyclo-oxygenase-(COX)-inhibiting nitric oxide donator, NMDA (N-methyl-D-aspartic acid) Receptor antagonist, an Acetylcholinesterase inhibitor, a HT Agonist and a Proton Pump Inhibitor for treating a patient in need thereof and a method of treating a human comprising administration of such combination dosage forms of axomadol and at least one second active agent.
US20050075268 cell is contacted with a photosentistising agent, cell is irradiated with light to activate photosentisitising agent, the cell is contacted with the molecule to be introduced, particularly for use in cancer treatment, gene therapy and vaccination The present invention provides a method for introducing a molecule into the cytosol of a cell in which the cell is contacted with a photosentistising agent, the cell is irradiated with light of a wavelength effective to activate the photosentisitising agent and, substantially at the same time or after the irradiation, the cell is contacted with the molecule to be introduced, particularly for use in cancer treatment, gene therapy and vaccination.
US8298521 Treatment for eye disorder The present invention relates to altering the physical and/or chemical properties of at least part of at least one tissue in the eye. In a specific embodiment, it relates to the treatment of any eye disorder, although in particular embodiments the individual has a thickened Bruch's membrane. An activating energy source is utilized to effect a controlled diffusion enhancement and/or degradation of Bruch's membrane that enables improved diffusional transport between the choroid and retina. The individual is administered an inactivated diffusion-enhancing molecule that becomes associated with the membrane, which is then precisely exposed to an activating energy source, such as light or ultrasound.
CN103191066A Dimethyl-sulfone-contained biodegradation microsphere and preparation method thereof The invention provides a dimethyl-sulfone-contained biodegradation microsphere and a preparation method thereof. The method comprises the following steps of dissolving dimethyl sulfone into a first organic solvent to obtain a first mixed solution; dissolving biodegradable macromolecules into a second organic solvent to obtain a second mixed solution; mixing the first mixed solution and the second mixed solution, pressing the mixed solution into a continuous phase through a film, and continuously stirring the mixed solution to obtain the dimethyl-sulfone-contained biodegradation microsphere. Compared with the oral dimethyl sulfone, by utilizing the biodegradable effect of the biological degradable macromolecules in a human body, the action time of the dimethyl sulfone in the body can be prolonged, the burst phenomenon of the dimethyl sulfone can be solved, a slow release effect can be realized, the action time of a drug can be increased, the time of taking medicine can be reduced, and the utilization effect of the dimethyl sulfone also can be improved; and by adopting a film emulsification technology, and the biological microsphere containing the dimethyl sulfone is enabled to have good consistency and drug loading capacity.
US20050277657 Method of protection of biologically active essential oils and pharmaceutical composition for weight control and enhance fat burning in adults, adolescents and children The subject of this invention is overweight and obesity. The invention relates to use of several natural sources of essential oils such as Cinnamon, Ginger and Turmeric oils. Additional compounds are Citric acid as a fat dissolver and Cocoa extract as an energizer. Especially developed technology is necessary to be used for manufacturing this product. In the first phase powders are separately mixed with oils that are added to inferior carriers (cellulose) to prevent reaction. At the end, Citric acid and Cocoa powder is added as an energizer. The final product Slimtrax® will be in a tablet form and will have appetite suppressant, fat burner and energizing effect. Product should be taken 15 minutes before the main meal with a large (8oz.) glass of water.
EP2277515A1 Use of the combination of teriflunomide and interferon beta for treating multiple sclerosis This invention is related to the use of the combination of teriflunomide or a pharmaceutically acceptable salt thereof and interferon beta-1a or 1 b for treating multiple sclerosis.
EP1572209A1 Novel quinoxalinone derivatives as bradykinin b1 antagonists 2-Quinoxalinone derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
WO2008067481A1 Aza-indolyl compounds and methods of use The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
CN103356575A Application of Sarcaboside A in preparation of drug for treating prostatic cancer The invention discloses application of Sarcaboside A in preparation of a drug for treating prostatic cancer, which belongs to the technical field of new applications of drug. According to the invention, the in-vitro MTT (Methyl Thiazolyl Tetrazolium) antitumor activity evaluation discovers that Sarcaboside A also has an obvious inhibiting effect on the growth of human prostatic cancer cell strains ALVA, gpc-1, 9L-B and Du145. Thus, Sarcaboside A can be used for preparing an anti-prostatic cancer drug and has good development and application prospects. The application of Sarcaboside A in preparation of the drug for treating prostatic cancer is disclosed by the invention for the first time. The skeleton type is brand new and Sarcaboside A has unexpectedly high inhibitory activity inhibitory activity on the human prostatic cancer cell.
CN103301107A Application of luteolin in preparation of medicament for treating and preventing stomach cancer The invention relates to the application of luteolin in the preparation of a medicament for treating and preventing stomach cancer. The luteolin can inhibit the proliferation of BGC-823 cells in vitro; the half inhibitory concentration (IC50) is 37.88+/-5.81 mu mol/L; and a flow cytometry detects that the luteolin can retard the BGC-823 cells in a G2/M stage and induce the apoptosis of the cells. Real-time quantitative polymerase chain reaction (PCR) detection shows that, after acting on the BGC-823 in vitro, the luteolin can promote the expression of the genes of dual-specificity phosphatase 1 (DUSP1), dual-specificity phosphatase 2 (DUSP2), dual-specificity phosphatase 4 (DUSP4) and dual-specificity phosphatase 5 (DUSP5) and inhibit the expression of a CXCL16 gene serving as a chemotactic factor; westernbloting detects the expression of protein p-ERK and Akt; after acting on the BGC-823 in vitro, the luteolin can inhibit the expression of the protein p-ERK and Akt so as to inhibit the overhigh activity of the pathways of MAPK and Akt; and therefore, the effect of treating tumors is achieved. A prevention model for the stomach cancer in a nude mouse is established; the luteolin can prevent and inhibit the growth of the tumors in vivo; immunohistochemistry proves that the expression amounts of the protein HIF-1 alpha, vascular endothelial growth factor (VEGF) and MMP9 are obviously reduced and can inhibit the generation of tumor vasculature in vivo; and therefore, a theoretical foundation is provided for the new application of the luteolin in the preparation of the medicament for treating and preventing the stomach cancer.
US7214368 Therapeutic regimen for treating cancer comprising the administration of adenoviral vectors comprising a TNF-α transgene The invention provides a method for treating a tumor in a human comprising administering to the tumor a dose of a pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier and (ii) an adenoviral vector comprising a nucleic acid sequence encoding TNF-α operably linked to a promoter, wherein the dose comprises about 1×107 to about 4×1012 particle units (pu) of replication-deficient adenoviral vector, at least once in a therapeutic period comprising up to 10 weeks, whereby the tumor in human is treated.
CN101690740A Calculi dissolving agent for treating urologic calculi The invention relates to a calculi dissolving agent for treating urologic calculi, belonging to the drugs for treating urologic calculi. The calculi dissolving agent comprises the following raw materials in percentage by weight: 5% of citric acid, 3% of ammonium molybdate, 2% of N-acetyl-D-glucosamine, 2% of panax notoginseng saponins, 20% of crystal sugar and the balance water. The calculi dissolving agent has the effects of softening calculi, dissolving calculi quickly, producing no simulation to urethra when the calculi are expelled, alleviating the pains of the patients and contributing to quick recovery and good treatment effects.
US7795280 3-(2-Nitro-phenylsulfanyl)-1-pyridin-2-ylmethyl-1H-indole-6-carbonitrile, used for the treatment of benign prostate hyperplasia, bone disorders, female sexual dysfunction,, atherosclerosis, anemia, muscular atrophy, as contraceptives or for hormone replacement therapy This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula or a salt or hydrate form thereof.
US20100099776 Oily suspension of atovaquone The present invention relates to an oily suspension of atovaquone comprising atovaquone particles and a combination of surfactants having HLB more than 10.
CN102688246A Phlomis umbrosa root total-drop triterpene composition and extraction method and application thereof The invention discloses a phlomis umbrosa root total-drop triterpene composition which comprises six concrete-drop triterpene compounds derived from the general formula A, and the formula shows the six major ingredients of the phlomis umbrosa root total-drop triterpene composition extracted in the invention. The in-vitro anti-tumor cell test indicates that: the phlomis umbrosa root total-drop triterpene composition disclosed by the invention has a relatively strong effect on suppressing tumor cells, and can be further developed and utilized as a candidate anti-tumor medicine, thereby laying a foundation for the further development and research.
CN1994382A Diet composition combined by blueberry, levo-carnitine, spirulina and lotus leaf The invention relates to a fat-reducing drug which uses blueberry, left-handed rotation carnitine, spirulina and lotus leaf, which can be made into health-care food or drug, wherein the invention can avoid loose bowel movement and anorexia. And youth can take it reduce fatty and improve learning ability; olds can take it to eliminate free radical and treat abnormal metabolism.
EP1492778A1 (4,2-disubstituted-thiazol-5-yl)amine compounds as pde7 inhibitors A compound selected from those of formula (I), wherein R1a, R1b, R2, R3 are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of phosphosdiesterase-7 (PDE-7).
CN103719142A Disinfectant as well as preparation method and application thereof The invention discloses a disinfectant as well as preparation method and application thereof. The disinfectant comprises following ingredient B and ingredient A: the ingredient B: organic boric acid and/or organic borate; the ingredient A: quaternary ammonium salt type cationic surfactant, wherein, the hydrophobic group contains at least ten carbon atoms, and the hydrophilic base is a cation containing nitrogen atom. The disinfectant provided by the invention has strong sterilization capability, and the sterilization efficiency can reach to 99.9999%. The disinfectant has little corrosivity, irritation and toxicity to surface of object and human body. The disinfectant can disinfect object surface and human body surface, and can disinfect contact lens and medical apparatus, thereby preventing propagation of microorganism in population by contact between human and object, and overcoming the disadvantages that the present product has strong irritation and low bactericidal activity for human body.
US7138142 Producing isoleucine, leucine and valine containing particles having reduced bitterness and odor; small volume dose The problem of the present invention is to provide pharmaceutical granules containing, as active amino acid ingredients, three kinds of branched chain amino acids of isoleucine, leucine and valine, which has a smaller specific volume than conventional products, and a production method thereof. As a result of intensive studies, granules containing, as active amino acid ingredients, three kinds of branched chain amino acids of isoleucine, leucine and valine and a production method thereof have been provided, which are characterized by adding an acid to a particle mixture of three kinds of branched chain amino acids of isoleucine, leucine and valine and granulating the mixture, which has solved the above-mentioned problem.
EP1224172B1 Drugs for the treatment of malignant tumours The invention relates to the use of compounds of general formula (I) or any tautomer, optical isomer or racemate thereof for the manufacturing of a medicament for the treatment of cancer. The invention also comprises novel compounds, pharmaceutical compositions, and processes for the preparation of the compounds of formula (I).
US20100256175 Treatment for drug addiction The invention discloses a method of treatment for drug addiction, comprising administering a therapeutic agent to a patient. The therapeutic agent is delivered in an inactive state and is converted into its active form in the presence of a narcotic. The conversion produces at least one unpleasant side effect for the patient. The therapeutic agent is implanted in the form of a depot, and maybe a prodrug or microspheres. The agent may be injectable or may be packaged in the form of bioerodible sticks. The agent may also be delivered via a surgical method. The disclosed method can also be used to detect the consumption of a banned substance.
EP2675790A1 Substituted 1, 2, 3, 4-tetrahydroquinolin-7-yl carbamates as acetylcholinesterase inhibitors for treatment of alzheimer's disease The present invention relates to novel substituted 1,2,3,4-tetrahydroquinolin-7-yl carbamates, their preparation, and use as therapeutic agents, particularly in the prevention or treatment of neurodegenerative or Alzheimer's disease, or senile dementia, or memory disturbances, and more particularly to the prevention, treatment and amelioration of Alzheimer's disease with the novel substituted 1,2,3,4-tetrahydroquinolin-7-yl carbamates, which act as inhibitors of central cholinesterase enzymes, particularly acetylcholinesterase (AChE) following the indirect cholinomimetic pathway. The present invention particularly relates to compounds of formula A: Formula A wherein R1=alkyl, aryl, substituted aryl; R2=H, methyl; R3=H, alkyl, alkenyl, alkynyl, aralkyl, substituted aralkyl, aryl, heteroaryl.
CN102898381A Amine salts of a CRTH2 antagonist Provided are amine salts of {4,6-bis(dimethylamino)-2-(4-(4- (trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl} -acetic acid, processes for their preparation, pharmaceutical compositions containing them, and their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease.
WO2013180140A1 Dihydroorotic acid dehydrogenase inhibitor The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor that is applicable to various diseases. As an active ingredient, a compound represented by formula (I) (wherein X represents a halogen atom; R1 represents a hydrogen atom; R2 represents an alkyl group having 1 to 7 carbon atoms; R3 represents -CHO; and R4 represents -CH2-CH=C(CH3)-R0 (wherein R0 represents an alkyl group having 1 to 12 carbon atoms which may have a substituent on a terminal carbon atom and/or a non-terminal carbon atom, or the like)), an optical isomer of the compound, and a pharmaceutically acceptable salt of the compound or the optical isomer. The compound, the optical isomer and the pharmaceutically acceptable salt have an excellent inhibitory activity on dihydroorotic acid dehydrogenase and therefore can be used as an immunosuppressive agent, a therapeutic agent for rheumatism, an anti-cancer agent, a therapeutic agent for rejection response, an anti-viral agent, an anti-H. pylori agent, a therapeutic agent for diabetes and the like.
CN101190201A Folic acid chewable tablets for dog or cat The invention discloses a folic acid chewable tablet used for dogs and cats. The invention can overcome the disadvantage of the poor palatability of the existing tablets, promote dogs and cats to chew and adsorb fully, effectively ensure the dosage of administration, enhance the cure rate of feline or canine diseases and reduce the waste of medicine. The tablet of the invention includes the following components represented by weight-percentage respectively: 1-5 percent of aspartame, 20-30 percent of the mixture of oral glucose and skim milk powder, in which the ratio of oral glucose and skim milk powder is 1:1-1:4, 40-60 percent of excipient, 0.5-1 percent of glidant and 10-30 percent of folic acid.
US20050004126 Method of determining potential allosterically-binding matrix metalloproteinase inhibitors Compounds are provided that bind allosterically to the catalytic domain of MMP-13 and comprise a hydrophobic group, first and second hydrogen bond acceptors and at least one, and preferably both, of a third hydrogen bond acceptor and a second hydrophobic group. Cartesian coordinates for centroids of the above features are defined in the specification. When the ligand binds to MMP-13, the first, second and third (when present) hydrogen bond acceptors bond respectively with Thr245, Thr 247 and Met 253, the first hydrophobic group locates within the S1′ channel of MMP-13 and the second hydrophobic group (when present) is relatively open to solvent. The compounds specifically inhibit the matrix metalloproteinase-13 enzyme and thus are useful for treating diseases resulting from tissue breakdown, such as heart disease, multiple sclerosis, arthritis, atherosclerosis, and osteoporosis.
US8110367 Methods for diagnosing renal disorders The present invention relates to methods for diagnosing the presence and progress of pathologies characterized by an accumulation of the extracellular matrix components by measuring the level of Connective Tissue Growth Factor (CTGF) in a sample. The method of the present invention is directed to diagnosing kidney fibrosis and associated renal disorders, in particular, complications associated with diabetes, hyperglycemia, and hypertension.
US20120027852 Pharmaceutical composition containing a "limus" family immunosuppressive macrolide A pharmaceutical formulation includes a Limus family immunosuppressive macrolide on a pharmaceutically acceptable excipient, which may be compounded as suitable for oral administration.
US8198435 Crystal form of N-benzoyl-staurosporine The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.
US20110021604 Methods and compositions for the specific inhibition of kras by asymmetric double-stranded rna This invention relates to compounds, compositions, and methods useful for reducing KRAS target RNA and protein levels via use of Dicer substrate siRNA (DsiRNA) agents possessing asymmetric end structures.
EP1207886B1 Sphingomyelinase inhibitors as agents with antiapoptotic and antiseptic action The invention relates to pharmaceutical compositions with antiapoptotic and antiseptic effect that can be used as inhibiting substances of sphingomyelinase. The inventive pharmaceutical compositions are particularly useful for the treatment of septicemia, arteriosclerosis, neurodegenerative diseases such as Alzheimer's disease, and retroviral infection such as HIV infections.
CN102949349A Stable xanthophyll preparation The invention provides a stable xanthophyll preparation and a preparation method thereof. According to the invention, xanthophyll is loaded into microspheres such that a stabilizing purpose is reached. A microsphere substrate is selected from starch, albumin, gelatin, chitosan, or ethyl cellulose. The xanthophyll microspheres provided by the invention are prepared through an emulsification solvent diffusion method. The xanthophyll microspheres have the advantages of round and neat appearance, no adhesion, and uniformly distributed particle size. Free xanthophyll microsphere preparation can be achieved under normal temperature. The operation is simple and feasible. With the method, a problem of raw material medicine loss during a preparation method adopting a spray-drying method is avoided.
WO2007003536A1 Substituted glycinamides having an antithrombotic and factor xa-inhibiting effect The invention relates to novel substituted glycinamides of general formula (I), wherein D, M, R3, R4, and R5 are defined as indicated in the description, the tautomers, enantiomers, diastereomers, mixtures, and salts thereof, especially the physiologically acceptable salts thereof with inorganic or organic acids or bases, which are provided with valuable characteristics.
WO2014152114A1 Heteroaromatic compounds as btk inhibitors The present invention encompasses compounds of the formula (I), wherein the groups X and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
US7034055 2-aminoindane analogs The present invention relates to therapeutically active 2-aminoindane analogs of formula (I): Also provided is a method of preparing compounds of formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.
CN101856359A Medicine compound against acute myeloid leukemia The invention discloses a medicine compound against acute myeloid leukemia; each unit dose of the medicine compound contains 2mg of all-trans-retinoic acid, 1 to 2mg of megestrol acetate, 100 to 200mg of bezafibrate and a carrier acceptable of medical science, and the mass ratio of megestrol acetate to bezafibrate is 1:100. The medicine compound can significantly improve the survival rate of patients with acute myeloid leukemia, and can open up a new way for clinical treatment.
CN101095801A Liquid for healing nanometer argentum dermatosis and method for preparing the same Disclosed is a rehabilitation liquid for treating skin diseases by employing nano silver and its preparing process, wherein the liquid is prepared from nano silver micro powder, freeze-dried aloe powder and distilled water through steps of mixing and stirring.
US20100137437 Composition for Inactivating an Enveloped Virus The present invention relates generally to the field of prevention of diseases caused by enveloped viruses. More particularly, this invention concerns a composition for inactivating an enveloped virus comprising at least one non phospholipid Lipid Vesicle (nPLV) able to interact with said enveloped virus and an agent that enhances the lipid exchange between said nPLV and the membrane of said enveloped virus.
CN1562005A Medicine special for gastric disease An internally-applied in the form of capsule for treating senile gastrosis, gastritis, gastric ulcer, gasroptosis, enteritis, etc is prepared from roptazol and benzylbenzoimidazole hydrochloride through proportional mixing, grinding, sieving, sealing in bottle for 3-7 days and loading in capsules.
US20090149799 Method for chemical modulation of neural activity Methods and related systems for modulating neural activity by repetitively blocking conduction in peripheral neural structures with chemical blocking agents are disclosed. Methods and systems for reversing effects of chemical blocking agents and/or for producing substantially permanent conduction block are also disclosed.
US7781408 Oral administration of gangliosides including 50% ganglioside GD3 as anticholesterol and antiinflammatory agents; decreased intestinal absorption of cholesterol; mediating inflammation of the intestine, retina or neural tissues; liquid or food suppliment for infants The invention provides formulations for mediating inflammation and for lowering blood cholesterol. For example, inflammation of the intestine, retina or neural tissues, may be mediated. Further the formulations are effective in decreasing blood cholesterol absorption. The formulations comprise at least one ganglioside, which may be selected from the group consisting of: GD3, GM1, GM2, GM3, GD1b, NANA, and sialic acid. The invention further provides a method of treating or preventing inflammatory diseases by delivery of at least one ganglioside to a subject in need thereof, and a method of reducing blood cholesterol in a subject be delivery of a ganglioside-containing formulation. The formulation of the invention may be used to supplement foods or liquids, and may for example be used in preparation of infant formula or foods.
US20090062323 Deuterium-enriched irinotecan The present application describes deuterium-enriched irinotecan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2013150036A1 Novel thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof The present invention relates to compounds of formula (I): wherein R6 is -CONH2 or a -C(Rα)(Rβ)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.
US20120172289 Multifunctional glycopeptide antibiotic derivatives for fluorescent imaging and photoactive antimicrobial therapy The present invention relates to a compound of formula (I) and compositions thereof, methods of their production as well as methods for treating bacterial infection.
WO2010149685A1 New compounds, pharmaceutical composition and methods relating thereto New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2, X3, X4, Y1, Y2, A, R1, R2, R3, R4, m, n, p, and q are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof in a patient in need thereof.
CN1721004A Biological active antibiotic dressing The invention provides an antibiotic dressing with bioactivity which comprises matrix material, and thin film agent, gelling agent, foam and particulate medicament thereon. the constituents of the medicament include silver oxide, silver peroxide and biological macromolecular compounds, wherein the biological macromolecular compounds include collagen, epidermal growth factor microspheres (EGF-PLGA), hyaluronic acid, heparin, chondroitin sulfate and alginates. The matrix material comprises woven fabrics, knit-woven fabrics or nonwoven fabrics made of animal skin materials and various fibrous materials. The dressing can be used for the treatment and/or prevention of burn and scald infection, bedsore, venous ulcer, diabetic ulcer, surgical operation infection, wound infection, acne, acne, ringworm of the nails and acarid infection.
US20080249154 Preventive and/or Therapeutic Agent For Disease In Which Mitochondrial Benzodiazephine Receptor Participates A compound represented by formula (I) (wherein ring A is a nitrogen-containing ring which may have a substituent(s), E is a binding bond or a spacer of which main chain has an atom number of 1-8, Q is a hydrogen atom, a hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s).), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. Since the compounds of the present invention represented by formula (I), a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof have the affinity to MBR, they are useful for the prevention and/or treatment for disease caused by stress.
WO2014135028A1 Pyridopyrimidine or pyrimidopyrimidine compound, preparation method, pharmaceutical composition and use thereof The present invention relates to the field of pharmaceutical chemistry. In particular, the present invention relates to a pyridopyrimidine or pyrimidopyrimidine compound as represented by general formula (I), or an isomer thereof or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof, a preparation method, a pharmaceutical composition and uses thereof in preparing an mTOR inhibitor. As the mTOR inhibitor, the compound or the pharmaceutical composition thereof can be used for treating the diseases or symptoms due to PI3K-AKT-mTOR signal path malfunction.
US7148245 Skin disorders; aging resistance of skins; antiinflammatory agents; antiallergens; rheumatic diseases; cardiovascular disorders Compounds of formula (I): in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2 and R3 represent, in particular, H or alkyl, or R2 and R3, taken together, form a 5- or 6-membered ring, R4 and R5 represent, in particular, H or halogen, R6 represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.
EP1220852B1 Substituted diazepans The invention provides novel diazepanes having interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1, -ICAM-2 or -ICAM-3 interactions.
US20100093673 Pain relieving patch Described here are patches for the treatment of pain. The patches include a carrier material, which itself, in the absence of an active agent, is capable of relieving pain. Methods of treating pain using the patches are also described.
US20080167264 Materials and methods to inhibit hodgkin and reed sternberg cell growth Materials and methods are disclosed for modulating proliferation of cell types associated with Hodgkin's disease through inhibition of IL-13 and components in IL-13 associated signal transduction pathways. Methods to identify inhibitors, compositions comprising the inhibitors, and methods using the inhibitors to treat Hodgkin's disease are also disclosed.
US20110257271 Derivatives of dimethylcurcumin The invention relates to compounds of Formula I or Ia as disclosed herein: or pharmaceutically acceptable salts thereof or tautomers thereof.
CN1864676A Prescription of mecillinam composite preparation for injection and preparation method thereof The present invention provides compound mecillinam sodium preparations for injection and aims at overcoming the inferior effect on some bacteria of single mecillinam sodium injection. The compound mecillinam sodium preparations for injection include amoxicillin sodium/ mecillinam sodium injection, ampicillin sodium/ mecillinam sodium injection and piperacillin sodium/ mecillinam sodium injection. The compound mecillinam sodium preparations for injection have synergistic effect, raised antibacterial effect, broader antibacterial spectrum, low toxicity, high safety and stable property.
CN102000108A Gynaecological medicine composition as well as external-use capsule and application thereof The invention relates to a gynaecological medicine composition as well as an external-use capsule and application thereof. The gynaecological medicine composition mainly comprises the following components in 1000 parts by weight: 2-20 parts of polyhexamethylene guanidine (PHGM), 1-30 parts of water and the balance of glycerol. The gynaecological external-use capsule comprises medical soft capsule and a medicine composition contained in the medical soft capsule, wherein the medicine composition comprises the following components in parts by weight: 2-20 parts of polyhexamethylene guanidine (PHGM), 1-30 parts of water and the balance of glycerol. The gynaecological medicine composition can be used for preparing antibacterial and antiphlogistic medicines for treating gynaecological diseases. The gynaecological external-use capsule has wide effects of resisting bacteria, thoroughly killing various bacterial viruses, eliminating inflammations and treating the gynaecological diseases; the gynaecological external-use capsule has good moisturizing effect, has the functions of keeping female skin soft, delaying and resisting skin aging and restoring damaged skin, and has no toxic and side effect.
EP2723331A2 Non-leaching antimicrobial wound dressing The present application discloses preparations of antimicrobial wound dressings. Strongly binding polymeric dialkyi aminoalkyi (meth)acrylates are used to treat highly absorbent wound dressing materials. The resulting finish is highly antimicrobial effective and non- leachable.
US20050003003 Modulation of release from dry powder formulations Particles which include a bioactive agent are prepared to have a desired matrix transition temperature. Delivery of the particles via the pulmonary system results in modulation of drug release from the particles. Sustained release and/or sustained pharmacologic action of the drug can be obtained by forming particles which include a combination of phospholipids that are miscible in one another and have a high matrix transition temperature.
WO2013138396A1 Dihydropyridopyrimidine and dihydronaphthyridine derivatives as tyrosine kinase inhibitors of especially vegf and pdgf The present invention relates to compounds of formulae I and II wherein the variables are as defined herein. These compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
CN103476407A Treatment of HER2-positive cancer with paclitaxel and trastuzumab-MCC-DM1 The present invention relates to combination therapy with paclitaxel, trastuzumab-MCC-DM1 and optionally, pertuzumab.
US7939540 4-(3-benzoylaminophenyl)-6,7-dimethoxy-2-methylaminoquinazoline derivatives A compound represented by the following formula (I), salt thereof, or hydrate thereof, can effectively relieve itch caused by atopic disease or the like: wherein R represents hydroxyl, C1-6 alkoxy optionally substituted with C1-6 alkoxy, or amino optionally substituted with C1-6 alkyl.
CN101103962A Vinpocetine oral self-micro-emulsification medicine-releasing system and preparation method thereof The invention relates to a vinpocetine oral self-micro-emulsifying drug delivery system and the preparation method. The vinpocetine oral self-micro-emulsifying drug delivery system is composed of vinpocetine, fat phase, emulsifier and coemulsifier. The mass ratio percentage preferential scope of the ingredients is that the vinpocetine occupies 1-10 per cent, the fat phase occupies 20-60 per cent, the emulsifier occupies 25-70 per cent and the coemulsifier occupies 0-25 per cent. The vinpocetine oral self-micro-emulsifying drug delivery system can be spontaneously emulsified into micro-emulsion with 10-100 mm granule diameter after taken orally, promoting drug to be quickly absorbed. The drug delivery system has the advantages of improving the solubility of the vinpocetine in water, improving the availability of the vinpocetine and eliminating the influence of food to the absorption and bioavailability of the vinpocetine.
CN103274953A Naphthol and o-naphthoquinone compounds thereof and preparation method and medical application thereof The invention relates to the field of biological medicine, and particularly relates to naphthol and o-naphthoquinone compounds thereof shown by the general formulas I and II or a pharmaceutically acceptable salt thereof or a medicinal carrier, a preparation method thereof, a medicinal composition containing the compounds and a medical application thereof, and particularly an application in preparing anti-tumor medicines. The results of pharmacological experiments indicate that the compounds have good anti-tumor activity and can be clinically used for preparing anti-tumor medicines.
CN103371979A Methylprednisolone sodium succinate freeze-dried powder injection The invention relates to a methylprednisolone sodium succinate freeze-dried powder injection. Every bottle of freeze-dried powder injection is prepared from 12-2550mg of methylprednisolone succinic acid, alkaline auxiliary material in which the sodium ion:succinic acid methylprednisolone mol ratio is 1:1, 0-200mg of excipient and pH value regulator. The powder injection is prepared by dissolving the components in the formula and carrying out freeze-drying. The invention is characterized in that the solvent is ethanol-containing water for injection, and the liquor prepared by dissolving the components in the formula in the solvent contains 5-10 vol% of ethanol.
US20090238866 Chewable capsules The invention provides an orally administrable chewable capsule comprising a capsule shell enclosing an oil-in-water emulsion in which the aqueous phase is gelled, or an oil droplet-containing dried residue of such an emulsion.
EP2389078A1 Dual cation dual anion coordination complexes Compounds are provided herein which are coordination complexes of the formula, AxByCit2Fz•mH2O, wherein A is a cation selected from certain IA or IIA metal ions in the Periodic Table; B is a cation selected from certain IIA metal ions and certain divalent d-block transition metal ions; A and B are different; "Cit" is tribasic citric acid anion; the stoichiometric ratio of x to y is equal or higher than 1.0 but lower than 8.0; m is 0-12; and z is selected such that electroneutrality is preserved. Compounds provided herein are useful to treat dietary deficiencies, osteoporosis, osteopenia, bone loss, and risk of bone loss, as well as other medical conditions involving the need for administration of the various ions. In addition, the compounds can be used as fluoride sources for dental use and to fluoridate water systems.
US20100125070 Bupropion Metabolites and Methods of Their Synthesis and Use Methods and compositions are disclosed which utilize metabolites of bupropion for treating disorders ameliorated by inhibition of neuronal monoamine reuptake. Such disorders include, but are not limited to, sexual dysfunction, affective disorders, cerebral function disorders, cigarette smoking, and incontinence. Methods of making optically pure bupropion metabolites are also disclosed.
WO2012165610A1 Composition for maintaining or improving skin barrier function An oral composition for maintaining or improving a skin barrier function, characterized by containing taurine as an active ingredient; or an oral composition for preventing or ameliorating age-related wrinkling, characterized by containing taurine as an active ingredient.
US8748400 Use of ketogenic compounds for treatment of age-associated memory impairment This invention relates to the field of therapeutic agents for the treatment of Age-Associated Memory Impairment (AAMI). In particular, the present invention utilizes compositions comprising at least one compound capable of elevating ketone body concentrations in a mammal (e.g., ketogenic compounds), administered in an amount effective for treatment or prevention of loss of cognitive function caused by reduced neuronal metabolism in AAMI. In one embodiment, the composition includes medium chain triglycerides (MCT). In another embodiment, the compositions are administered in the presence of carbohydrate. The present invention also relates to oral dosage forms, in particular, a nutritional drink comprising at least one compound capable of elevating ketone body concentrations in a mammal.
WO2010112578A1 4 -isopropyl-3-methylphenol for the treatment of inflammation This invention relates to the use of 4-isopropyl-3-methylphenol (IPMP) for combating inflammation and compositions comprising IPMP for such use.
EP1738761A1 Preventive and/or remedy for inflammatory bowel diseases The present invention relates to a preventive and/or a therapeutic agent for inflammatory bowel diseases containing a fermentation product of a propionic acid bacterium as an active ingredient.
US20110171203 Methods for treating neoplastic disease targeting o-linked n-acetylglucosamine modifications of cellular protein Methods for treating a neoplastic disease in a mammalian subject are provided. The method provides administering an inhibitor of O-GlcNAc transferase in an amount effective to reduce or eliminate the neoplastic disease in the mammalian subject. Method for diagnosing a risk factor for a neoplastic disease in a mammalian subject and methods for identifying a test compound which inhibits a hexosamine signaling pathway in a cell or tissue are provided.
US20100240709 Sulfoximine Derivatives as p38 MAP Kinase Inhibitors The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
EP1740172A2 Acetylcholinesterase inhibitors and n-methyl-d-aspartate antagonists useful in the treatment of cognitive disorders The present invention relates to compositions and methods of treating a cognitive disorder in a subject by administering an effective amount of phenserine or a pharmaceutically acceptable salt thereof and an effective amount of memantine or a pharmaceutically acceptable salt thereof to a subject, thereby treating a cognitive disorder in the subject.
WO2007037543A1 Biarylamide derivative Disclosed is a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 represents a heteroaryl group which may have a substituent or the like; R2 represents a lower alkyl group; R3 represents a heteroaryl group which has at least one nitrogen atom and may have a substituent or the like; X1 represents a carbon or nitrogen atom; ; X2 represents a carbon or nitrogen atom; and X3 represents a carbon or sulfur atom. The compound or the salt has an inhibitory effect on a metabotropic glutamate receptor 1, and therefore is useful for the treatment of a disease such as convulsion, acute pain, inflammatory pain, chronic pain, a gastrointestinal disorder, a brain disorder (e.g., cerebral infarction, transient cerebral ischemic attack), a mental dysfunction (e.g., schizophrenia), anxiety and drug dependence.
US7202366 Heterocyclic analogs of diphenylethylene compounds Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.
CN103417476A Menbutone injection liquid for veterinary use and preparation method thereof The invention discloses menbutone injection liquid for veterinary use. Every 100 ml of the menbutone injection liquid is prepared from: 10g of menbutone, 5.5g of diethanol amine, 0.2g of chlorocresol, 0.2g of sodium metabisulfite or sodium sulfite, 0.2g of edetic acid, and the balance of water for injection. The preparation method includes the steps of taking 45-55 ml of the water for injection, adding the diethanol amine into the water for injection to stir and mix evenly, adding the menbutone to stir until the mixture is fully dissolved at 50+/-5 DEG C, then adding the sodium metabisulfite or the sodium sulfite and the edetic acid, stirring the mixture to make the mixture dissolve, then adding the chlorocresol, stirring the mixture and making the mixture dissolve at 50+/-5 DEG C, cooling the mixture to indoor temperature, using the water for injection to carry out constant volume to 100 ml, mixing the mixture evenly, filtering the mixture through a millipore filter with a 0.45 micron pore diameter and a millipore filter with a 0.22 micron pore diameter in sequence, carrying out nitrogen charge, encapsulation and sterilization, and then obtaining the menbutone injection liquid for veterinary use. The prescription of the injection liquid is advanced, simple in process, good in repeatability, stable and effective in product quality, and the injection liquid prepared through the method is proper in PH value, and can be dosed through intramuscular injection or vein injection, fills the blank of cholagogue for veterinary use in China, and contributes to improve the level of drug use by veterinarians in China.
WO2008036312A1 Fungicidal methods using immune response modifier compounds The present invention provides methods of killing fungal cells using immune response modifier compounds. In one aspect, the method generally includes contacting an immune response modifier (IRM) compound with a fungicidal effector cell, thereby activating the fungicidal effector cell, and allowing the activated fungicidal effector cell to kill fungal cells. In another aspect, the method generally includes contacting a fungicidal IRM compound with fungal cells in an amount effective to kill fungal cells.
WO2008116816A1 Combination of cb2 ligand and paracetamol Combination of one or more CB2 modulators and paracetamol are useful of treating conditions which are mediated by the activity of CB2 receptors such as an immune disorder, an inflammatory disorder, pain, rheumatoid arthritis, multiple sclerosis, osteoarthritis, and osteoporosis.
CN103446066A Paroxetine liensinine freeze-dried powder and preparation method thereof The invention relates to a paroxetine liensinine freeze-dried powder, which is prepared from the following raw materials: 22 g of paroxetine, 16 g of tartaric acid, 8 g of citric acid, 48 g of polyethylene glycol 800, and 2000 ml of water for injection. The pH is adjusted to the range from 6.6 to 6.8.
EP0662128B1 Methods and compositions for controlling translation of hcv proteins Embodiments of the present invention feature methods and compositions for controlling the translation of viral peptides and proteins from viral nucleic acid, with particular applications to pestivirus and HCV. The methods and compositions feature control elements of the 5'UT region of the viral genome.
CN101756959A Nutritional composition for improving anti-stress ability of aquacultural animals, preparation method and applications thereof The invention relates to a nutritional composition for improving the anti-stress ability of aquacultural animals, wherein the composition comprises the following components in percentage by weight: 50 percent of vitamin C1; 50 percent of lactose 1; 50 percent of effervescing agent; and 30 percent of lubricant. The effervescing technology of the nutritional composition for improving the anti-stress ability of the aquacultural animals can effectively cause the nutritional composition to be rapidly disintegrated, thus, the invention has the advantages of convenient use, quick response and high bioavailability, and can improve the clinical curative effect.
US20070298096 Analgesic/Antipyretic Compositions for Enhanced Absorption The onset of activity of a first analgesic/antipyretic composition containing an analgesic/antipyretic effective amount of acetaminophen, caffeine and, optionally, aspirin is shortened by incorporating in the first composition an onset of analgesic/antipyretic activity shortening amount of at least one alkaline agent whereby a second composition is produced. The second composition being bioequivalent to the first composition but having a shorter onset of analgesic/antipyretic activity than the first composition.
US20080027044 Prodrug antibiotic screens Methods for identifying prodrug activity utilizing screens with microbial mutants, including null and conditional mutants, transiently gene-repressed microbes, and gene-overexpressing microbes, as well as pooled collections of these are provided. Effective prodrug antibiotics differentially kill or inhibit microbes overexpressing prodrug activating genes and allow non-expressing strains to grow and be readily identified. Methods for detecting prodrug antibiotic activity by detecting a lack of differential sensitivity of multidrug efflux mutant or deficient strains are also provided. Novel pharmaceutical compounds identified by the methods of the invention, pharmaceutical formulations, and methods for treating an infection comprising administering to a subject in need thereof an effective amount of a Compound of the Invention are also provided.
US20070232586 Hydrazino-Substituted Heterocyclic Nitrile Compounds and Use Thereof A compound having an inhibitory activity against cysteine protease, represented by formula (I): (wherein ring X is a heterocyclic group which may contain 1 to 4 hetero atoms selected from an nitrogen atom(s), a oxygen atom(s) and a sulfur atom(s) which may be oxidized, in addition to said nitrogen atom in the ring; J is a bond or a spacer having from 1 to 8 atoms; R, R1, R2 and R3 is each independently hydrogen atom or a substituent; n is 0 or an integer of 1 to 10), a salt thereof, a solvate thereof, or an N-oxide thereof, or a prodrug thereof; and an agent for prevention and/or treatment for a cysteine protease-related disease, such as osteoporosis, comprising it as an active ingredient are provided.
US20090306200 Prophylactic or Therapeutic Agent for Nocturnal Conduct Disorder Associated With Dementia The present invention provides a prophylactic or therapeutic agent for nocturnal conduct disorders associated with dementia, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide.
CN103301182A Plant chemome formula used by tumor patients The invention discloses a plant chemome formula used by tumor patients. The plant chemome formula is obtained according to a global systems biology method of integrating chemomics and is prepared by mixing polysaccharide plant chemomes, a saponin plant chemome and a protein plant chemome. The plant chemome formula and acceptable excipients can be prepared into health food, special diet food and the like in dosage forms of powder and capsules according to conventional processes. The plant chemome formula can promote red blood cells to eliminate immune complexes and promote autoimmune regulation capacity of the red blood cells, repair immune system damages caused by radiotherapy and chemotherapy, inhibit tumor metastasis and protect livers from being damaged by medicines, and is suitable for medical treatment protection of tumor people awaiting treatment after definite diagnosis, tumor people in the rehabilitative period and tumor people receiving radiotherapy, chemotherapy and operations and for medical nutrition intervention of terminal tumor people losing opportunities of operations, radiotherapy and chemotherapy.
CN103044409A Puerarin derivative or pharmaceutically acceptable salt and application thereof The invention discloses a puerarin derivative or pharmaceutically acceptable salt thereof. According to the defects of the prior art, the structure of puerarin is modified; the water solubility and lipid solubility of puerarin are improved by changing the size, shape and space structure of molecules, and meanwhile the pharmaceutical activity of puerarin is maintained; and the puerarin derivative or pharmaceutically acceptable salt thereof has a structure of the general formula I shown in the specification.
EP1506780A2 Pharmaceutical formulations with macrolides alone or mixed with other active agents Dispersible tablets containing 20 - 60 % by weight of a macrolid (I) and 1 - 25 % of a disintegration agent (II) together with a sweetening agent. - (I) is present as the base and is one or more of the following: pristinamycin, azithromycin, roxithromycin, clarithromycin, and spiramycin. The disintegrating agent (II) is preferably 1 - 16 % polyvinyl pyrrolidone, 1 - 15 % sodium croscarmellose or a 1:1 - 4:1 mixture of these two. The sweetening agent is preferably aspartame, sodium saccharin, potassium acesulfame, ammonium glycerinate, or their mixtures. The tablets may further contain an active nitro-imidazole, especially metronidazole, tinidazole or ornidazole, as well as conventional diluents, surfactants, lubricants, flow agents and flavors. - ACTIVITY - Antibiotic. - MECHANISM OF ACTION - None given.
CN101229121A Penciclovir microemulsion gel preparation and preparing method thereof The invention relates to a penciclovir micro-emulsified gel and preparation process, belonging to medicine technology field, which comprises penciclovir surfactant, assistant surfactant, oil phase, water and carbomer and is used for transdermal drug delivery, the processing method is simple, the quality is easy to be controlled, and the stability of the gel is good, compared with present cream, the unit area accumulation infiltration amount of drugs can be improved obviously, and detained dosage in epidermis and dermis can be improved, moreover the invention has certain sustained-release function so that drug treating times and drug amounts can be reduced, and the using process of the drug is convenient, no pollution is caused to clothes, so the medicine is suitable for clinical wide application.
EP2611919A2 Kinases as targets for anti-diabetic therapy The present invention is related to compound capable of modulating the activity and/or expression of the protein kinases SCYL1, ADCK1, GRK5 and CSNK2A1, thereby enhancing the expression and/or release of insulin. The invention is further related to methods of identifying said compounds for the treatment of metabolic diseases. The invention is further related to methods of treatment of metabolic diseases, particularly diabetes mellitus type 2.
WO2014060509A1 Use of a bioactivated phytochemical as a neuroprotective agent for preventing and treating disorders related to nervous system The use of a bioactivated phytochemical is disclosed for preventing and treating neurodegenerative diseases, such as Parkinson's disease and multiple sclerosis. In particular, said bioactivated phytochemical is Rs-Glucoraphanin bioactivated with myrosinase and has proved to be particularly suitable as being surprisingly effective and extremely well tolerated by the body.
CN101812033A Ibuprofen 2-arylmorpholine ethyl ester as well as preparation method and application thereof The invention discloses an ibuprofen 2-arylmorpholine ethyl ester or 2-arylmorpholine ethyl ester salt. The ibuprofen 2-arylmorpholine ethyl ester has the following chemical structural formula. A preparation method of the ibuprofen 2-arylmorpholine ethyl ester comprises the following steps of: dissolving ibuprofen acyl chloride into tetrahydrofuran, and reacting for a certain time by dripping a 4-hydroxyethyl group-2-arylmorpholine tetrahydrofuran solution under stirring; and distilling and recovering the tetrahydrofuran to obtain the ibuprofen 2-arylmorpholine ethyl ester. A preparation method of the 2-arylmorpholine ethyl ester salt (II) comprises the following steps of: dissolving the ibuprofen 2-arylmorpholine ethyl ester into anhydrous ether or ethanol; and accessing a dry HCl gas or reacting with a corresponding acide (HY) to obtain the 2-arylmorpholine ethyl ester salt (II). The 2-arylmorpholine ethyl ester or the 2-arylmorpholine ethyl ester salt (II) is applied to preparing an anti-inflammatory and analgesic drug.
WO2010001126A1 Thiophene derivatives as kinase inhibitors A series of thiophene derivatives which are substituted in the 2 -position by a morphoIin-4-yl substituent, and in the 3 -position by a substituted ethynyl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
WO2013154128A1 Novel arteriosclerosis treatment drug composition and method for screening arteriosclerosis treatment drugs The present invention pertains to: the use as the target of treatment for dyslipidemia, hyperlipidemia, arteriosclerosis, or Alzheimer's disease of a gene coding for the human CTNNB1, human NFE2L2, human TXN, human CUL1, human RAE1, human TNFRSF10C, human BCLAF1, human TNIP1, human STK38, human ZC3H13, human C14orf122, human C4orf18, human ARS2, human C4orf20, human RC74, human EP400, human RUFY1, human EPPK1, human SLA2, human FTMT, human GPR139, human OR10AG1, human C1QTNF9, human UBE2NL, human FLJ16734 or human FLJ38596 proteins; a treatment agent for dyslipidemia, hyperlipidemia, arteriosclerosis, or Alzheimer's disease targeting the genes; and a method for screening treatment agents for dyslipidemia, hyperlipidemia, arteriosclerosis, or Alzheimer's disease targeting the genes.
US8809326 Isoquinolinone Rho kinase inhibitors Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.
CN101585858A Application of glycosylated puerarin derivate and its combination for preventing and treating cardiovascular and cerebrovascular disease The invention relates to a glycosylated puerarin derivate shown in the general formula (I) and its pharmaceutically acceptable salt. In the formula, R is described as the text. A preparation method and a medicament combination containing the compound shown in the general formula (I) of the effective dose are also provided. The combination is used for treating and preventing the cardiovascular and cerebrovascular diseases, diabetic nephropathy and osteoporosis.
CA2449002C Enhancement of oral bioavailability of non-emulsified formulation of prodrug esters with lecithin A method for enhancing the oral bioavailability of a prodrug ester by formulating the ester as non-emulsified formulation with lecithin; as well as a pharmaceutical composition of at least one antibiotic and lecithin in a non-emulsified formulation; a method of treating infections with the non-emulsified formulation, and a method for preparing tablets by direct compression of blends of drugs with lecithin are disclosed. Non-emulsified formulations include solids, tablets, capsules, lozenges, suspensions, elixirs and solutions, and exclude emulsions, liposomes, lipid matrix systems and micro-emulsions. A suitable prodrug ester is a cephalosporin .szlig.-lactam antibiotic such as cefditoren pivoxil, and a suitable non-emulsified formulation is a solid formulation.
CA2532078A1 Naphthylene derivatives as cytochrome p450 inhibitors Compounds of the formula (I); and pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, G 1,Q1, Z, R1, R2, R3, R4a, R4b, R5a, and R5b are defined herein, inhibit the cytochrome P450RAI enzyme and are useful for the treatment and/or prevention of various diseases and conditions which respond to treatment by retinoids and by naturally occurring retinoic acid.
US7217705 synergistic effect; CB1 receptor antagonist is an azetidine compound of given formula such as N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide, and the dopaminergic agent is ropinirole or levodopa for example The present invention relates to the combination of one or more CB1 antagonist azetidine derivatives and of one or more products which activate dopaminergic neurotransmission in the brain, to the pharmaceutical compositions comprising them and to their use in the treatment of Parkinson's disease.
WO2007085204A1 γ-BUTYROLACTONE COMPOUNDS, THE PREPARATION METHODS AND MEDICAL USES THEREOF The present application has disclosed compounds as well as their racemes or their optical isomers and their pharmaceutically acceptable salts or solvates of formula (I),in which the definitions of substituents are illuminated as description. The present application has also disclosed pharmaceutical compositions containing the present compounds. The present application has also disclosed their preparation methods and uses in preparing for medicaments of antiobesity agents or antitumor agents.
EP1530478A2 Exemestane for first-line treatment of breast cancer Exemestane is disclosed for use in the first-line treatment of metastatic, advanced hormone-dependent breast cancer, particularly in post-menopausal woman.
CN103169667A Preparation method of multifunctional meso-porous silicon nano preparation carrying gossypol derivative The invention discloses a preparation method of a multifunctional meso-porous silicon nano preparation carrying a novel gossypol derivative ApoG2. The preparation method comprises the following steps of: adding a defined amount of meso-porous surfactant to a diluted strong base solution, stirring the solution, dropping TEOS (tetraethyl orthosilicate) and cyanine dye Cy5.5 into the solution which is heated to a certain temperature, reacting the solution for a period of time under the conditions of constant temperature and serious stirring, filtering the reaction product, and dialyzing the product for multiple times to prepare fluorescent-dye-doped meso-porous silicon matrix nano particles; and mixing the after centrifuged multifunctional nano particles with a solution of the novel gossypol derivative ApoG2, and oscillating, centrifuging and washing the mixture to obtain the traceable multifunctional meso-porous silicon nano preparation carrying the novel gossypol derivative ApoG2. The preparation method has the advantages of simple procedure, small particle diameter, high monodispersity, stable fluorescence property, high drug loading capacity and the like, thereby enabling the ApoG2 to better play a role in anti-tumor.
US20100260860 Methods for Treating Vasomotor Symptoms in Castrated Prostatic Cancer Patients with Low Dose Cyproterone Acetate The present invention is directed to methods of treating vasomotor symptoms in castrated prostatic cancer patients in need of treatment, comprising administering about 15 mg or less of cyproterone acetate per day to the patients. The present invention is further directed to dosage forms comprising about 1 mg to about 15 mg of cyproterone acetate and a package comprising a plurality of dosage forms comprising about 1 mg to about 15 mg of cyproterone acetate.
CN102698274A Medicine composition for treating intractable escherichia coli of fowls The invention provides a medicine composition for treating intractable escherichia coli of fowls. The medicine composition comprises the following components in weight percentage: 6-10 percent of Colinflosaxin, 24-32 percent of sodium carbonate, 2-4 percent of ciprofloxacin, 6-10 percent of intestinal repair agent and 40-60 percent of anhydrous sugar. After the medicine composition provided by the invention is used for treating the intractable escherichia coli for one course of treatment, the symptom disappears, and the cure rate reaches 98 percent.
EP1286967B1 Cyclohexane derivatives and their use as therapeutic agents The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R?1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b¿ are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
DE102006047156A1 Cosmetic or dermatological composition comprises 2-isopropyl-5-methylcyclohexylcarbonyl-D-alanine ethyl ester and a skin lightener Cosmetic or dermatological composition comprises 2-isopropyl-5-methylcyclohexylcarbonyl-D-alanine ethyl ester (I) and a skin lightener. - ACTIVITY : Dermatological. No biological data given. - MECHANISM OF ACTION : None given.
CN102764252A Application of valnemulin hydrochloride The invention provides an application of valnemulin hydrochloride which is utilized to prepare a medicine for treating and preventing chicken mycoplasma infection and bacterial infection diseases. The medicine prepared by the valnemulin hydrochloride is a premix, soluble powder and a solution. Compared with traditional technology, the valnemulin hydrochloride provided by the invention is applied to chicken respiratory disease and chicken bacterial infection disease, so that the treatment effect of the valnemulin hydrochloride is more significant and the two diseases can be completely healed under the reasonable dose; and the residual quantity of the medicine in the chicken bodies is very low after the chicken is healed, the healed chicken is free from drug resistance of the medicine, so that the medicine can be repeatedly utilized but the curative effect of the medicine is not influenced.
US20090074837 Bioresorbable Calcium-Deficient Hydroxyapatite Hydrogel Composite The present invention provides a composite material comprising oxidized bacterial cellulose and calcium-deficient hydroxyapatite, and methods for preparing the composite material. The composite material is useful as a bone graft material. In another embodiment, the invention provides a method for tissue repair in a mammal. The method comprises inserting the composite material into cartilage or bone tissue.
WO2014024518A1 Filaggrin gene expression promoter Provided is a novel substance that promotes the expression of the filaggrin gene involved in improving the moisture retention function of skin. The filaggrin gene has been discovered to increase and decrease in expression with a rhythmicity of an about 24-hour period. Candidate substances were added; the candidate substances were then screened at the time when expression was at a maximum; and Japanese pepper extract, 3-(1'-piperidine)-propionic acid, geranium oil, cypress oil, rose oil, galbanum oil, pepper oil, basil oil, methyl o-toluate, methyl anthranilate, and dimethyl anthranilate were identified as filaggrin gene expression promoters.
WO2007047576A1 Pharmacological treatments for sleep disorders This invention is directed to methods for preventing or ameliorating sleep-related breathing disorders. The method comprises administration to a patient in need thereof an effective dose of one or more antitussive agents. The antitussive agent or combination of antitussive agents can be administered in conjunction with one or more serotonin receptor agonists, one or more cannabinoid receptor agonists, one or more serotonin reuptake inhibitors, a combination of reuptake inhibitors, other agents, or any combination of the foregoing.
US20100069402 Treatment of Behavioral Disorders The present invention relates to a method for treating a behavior disorder comprising the administration of a therapeutically effective amount of antihistamine, such as cetirizine, fexofenadine; loratadine, and desloratadine. The behavioral disorders may include ADHD, anxiety, depression, and autism. The method may include the administration of the antihistamine in combination with a stimulant medication, such as methylphenidate, thereby to achieve a synergistic effect. In any event, the amount of antihistamine and/or stimulant is effective to downregulate neurotrophic factors such as nerve growth factor or CD40. The invention is also directed to a method of preventing the onset of behavior disorders in patients presenting with symptoms of allergic rhinitis.
CN103239492A Production method of medicament for treating chicken asthma The invention discloses a production method of a medicament for treating chicken asthma and provides a medicament which is used for treating the chicken asthma with a quick acting effect. According to the technical scheme, the medicament is produced according to working procedures of boiling in water, mixing and packaging. The production method of the medicament for treating the chicken asthma comprises the following steps of: (1) selecting isatis root slices, putting the isatis root slices in a pot, adding water, and heating to decoct to obtain isatis root soup; (2) filtering the isatis root soup to obtain isatis root filtrate; (3) adding ambroxol hydrochloride to the isatis root filtrate, and uniformly stirring to obtain mixed medicinal liquor; and (4) carrying out vacuum package on the mixed medicinal liquor. According to the production method, the adopted production method is simple and convenient to operate; and the medicament produced by using the production method is quick-acting and can be easily ingested by chicken when used for the chicken asthma.
CN101504379A Medicinal smectite X-ray diffraction map identification standard The invention discloses an identification standard for an X-ray diffraction pattern of pharmaceutical montmorillonite, which is characterized in that characteristic spectral lines of the X-ray diffraction pattern of montmorillonite are positioned at wavelengths of about 1.5nm and about 0.45nm, and intensities of other impurity peaks in the pattern cannot be higher than a second characteristic peak (at about 0.45nm wavelength) of the montmorillonite, wherein the sum of the intensities of two impurity peaks at wavelengths of about 0.40nm and about 0.3nm cannot be higher than the second characteristic peak (at about 0.45nm wavelength) of the montmorillonite.
US20080096947 Polyvinylpyrrolidone or cyclodextrin as a builder, and polysorbate as a wetting agent, are dissolved with imexon in an organic solvent, preferably dimethyl sulfoxide, and lyophylized; lyophilisates are dissolved in aqueous propylene glycol; improved storage stability The invention relates to intravenously highly compatible imexon injection preparations and processes for their production as well as imexon lyophilisates stable in storage for the production of the injection preparations.
US20110003780 Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof The present invention relates to the compound of the Formula I: and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. IM=105109
WO2013107609A1 Systemic administration forms with controlled release and improved stability The invention relates to a monoterpene-containing administration form for peroral administration in the form of a capsule, especially in the form of a capsule with core-shell structure with multilayer shell, with improved storage stability, and with improve mechanical, optical and tactile properties.
CN103450093A 2-aminobenzimidazoles and applications thereof The invention relates to the field of medicinal chemistry and particularly relates to 2-aminobenzimidazoles, preparation methods thereof, medicinal compositions with the 2-aminobenzimidazoles and medical applications of the 2-aminobenzimidazoles.
US20080025959 Permeability of blood-brain barrier This relates to a discovery of a cell surface protein, namely NgR2, that is implicated in regulation of blood-brain barrier (BBB). In addition, the invention relates methods for identifying agents that modulate BBB permeability. Furthermore, the invention relates to methods of delivering therapeutic agents to the central nervous system by increasing BBB permeability.
EP2659884A2 Selective apoptotic induction in cancer cells including activation of procaspase-3 Compounds and related methods for synthesis, and the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3, and particular embodiments are capable of direct activation of procaspase-3 and procaspase-7 to the effector forms of caspase-3 and caspase-7. Procaspase-3 levels can vary among cancer cell types; several types have relatively high levels and can have increased susceptibility to chemotherapy by compounds and methods herein. Therapeutic applications are relevant for a variety of cancer conditions and cell types, e.g. breast, lung, brain, colon, renal, adrenal, melanoma, and others.
US20090069373 Quinoline Acids This invention relates generally to quinoline-based modulators of Liver X receptors (LXRs) and related methods.
CN101037420A New crystal type of netoglitazone and preparation method thereof Crystal form of nateglinide and its producing method are provided, relating to the chemical medicine field, especially to the medicine for treating diabetes. The X-radial powder diffraction spectrum of the crystal form of nateglinide has absorption peak at 14.9+-0.2, 17.3+-0.2, 18.4+-0.2, 19.0+-0.2, 19.5+-0.2, 20.4+-0.2, 22.1+-0.2, 24.2+-0.2, 25.2+-0.2, 26.7+-0.2, 27.7+-0.2 which is represented by 2theta. Crystal form of nateglinide has an absorption single peak at 148+-0.3 DEG C measured by DSC. The infra-red spectrum of the crystal form of nateglinide has absorption peak at 1757+-3cm-1, 1688+-3cm-1, 981+-1cm-1, 767+-1cm-1. The nateglinide F-crystal form has a good stability and can be produced in a large scale. The nateglinide F-crystal form produced from the complex form has a simple art, a convenient operation, and a similar drug action with the known nateglinide A-crystal form and does not gain special equipments.
WO2007022935A1 Azabicyclo [3.1.0] hexylphenyl derivatives as modulators of dopamine d3 receptors The present invention relates to novel compounds of formula (IA) or a salt thereof: Formula (IA), wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consisting of: -SO2NR5-, -SO2CR2R3-, - CR2R3SO2- and -NR5SO2-; R1 is hydrogen, C1-6alkyl, haloC1-6alkyl or C2-6alkylene; R2 and R3 are independently hydrogen or C1-6alkyl; R4 is hydrogen, halogen, C1-6 alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; R5 is hydrogen, C1-6 alkyl, or a phenyl optionally substituted by R4; and R6 is hydrogen, C1-6 alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
US8722672 Topical pharmaceutical composition including rel-N-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4′-(trifluoromethoxY)-[1,1′-biphenyl]-3-carboxamide The present invention relates to pharmaceutical compositions of 2-Methyl-4′-trifluoromethoxy-biphenyl-3-carboxylic acid [6-(cis-2,6-dimethyl-morpholin-4-yl)-pyridin-3-yl]-amide, to the use of such compositions in therapeutic applications and to methods for manufacturing such compositions.
EP1268431B1 3-cyanoquinolines,3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors Compounds of Formula (I), having the structure or a pharmaceutically salt thereof are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.
EP1353687B1 Methods for obtaining inhibitors of tirc7 ligand binding and uses thereof Provided are uses of agents interfering with the interaction of TIRC7 with its ligand such as HLA-(Human Leukocyte associated Antigen) class II alpha ( alpha ) chain for the preparation of pharmaceutical compositions for the treatment of graft versus host disease, autoimmune diseases, allergic diseases, infectious diseases, sepsis, for the treatment of tumors, for the improvement of wound healing or for inducing or maintaining immune unresponsiveness in a subject. In addition, methods for identifying and obtaining such agents are described. Furthermore, methods of diagnosing an immune disease or a tumor by determining the presence or absence of TIRC7 ligand are provided.
CN102846784A Paederia scandens water extract, and preparation method and application thereof The invention discloses a paederia scandens water extract containing an iridoid glycoside compound. The extract is characterized in that the iridoid glycoside compound contains 8.00-60.0% of paederosidie acid. The invention also discloses a preparation method of the paederia scandens water extract. The method comprises the steps that: (a) a paederia scandens material or decoction pieces are subjected to water extraction, such that an extraction liquid is obtained; (b) the extraction liquid is concentrated; methanol or ethanol is added, or the concentrated liquid is subjected to standing, and the liquid is precipitated; and a supernatant is obtained; (c) the supernatant is concentrated until no alcohol smell is left; the concentrated liquid is subjected to macroporous resin chromatography; elution is carried out sequentially by using water and ethanol of different concentrations; an eluant is collected; ethanol is recovered; and the eluant is subjected to reduced-pressure drying, such that the paederia scandens water extract is obtained; and (d) optionally, ethanol is added to the paederia scandens water extract obtained in the step (c), and filtering, concentrating, and drying are carried out. The paederia scandens water extract provided by the invention can be used for preparing medicines used for treating gout. The preparation method has simple processes, and is suitable for industrialized productions.
CN102698107A Figwort pill for clearing away internal heat and toxic materials The invention discloses a figwort pill for clearing away internal heat and toxic materials, which belongs to a novel technology for treating encephalitis invented by an applicant and is used for solving the problem that other medicaments cannot be used for curing encephalitis. According to a formula, the figwort pill comprises 15 types of Chinese medical herbs including (2-7)g of rhinoceros horn, (12-17)g of rehmannia root, (14-22)g of gypsum, (8-14)g of common anemarrhena, (8-14)g of weeping forsythia, (8-14)g of figwort, (4-10)g of dwarf lilyturf root, 2g of heart of lotus seed, (6-12)g of concha haliotidis, (2-8)g of tabasheer, (2-8)g of scorpio, (2-8)g of stiff silkworm and the like. The formula has the pharmacological effects of clearing away internal heat and toxic materials, clearing away internal heat and purging pathogenic fire, nourishing yin, cooling the blood, nourishing the stomach to improve the production of body fluid, detoxifying and resolving a mass. As proved by a part of cured cases, the figwort pill for clearing away heat and toxic materials is a unique effective novel technology for treating encephalitis invented by the applicant.
CN101032522A Medicine for curing herpes zoster The present invention discloses one kind of medicine for treating herpes zoster. The medicine is compound saponin glue prepared with Liushenwan pill (pill of six ingredients with magical effects), and compound aescin sodium gel in certain ratio, and through grinding Liushenwan pill into fine powder, and mixing with compound aescin sodium gel. The present invention has high healing effect, no side effect, low cost and other advantages.
CN101278905A Ophthalmic composition containing natamycin, use and preparation method thereof The invention discloses an ophthalmic composition containing natamycin, a usage and a preparation method; the composition contains: a) the natamycin, wherein, concentration of the natamycin is an effective antifungal concentration in eye region of mammals; b) one or a plurality of antimicrobial drugs, wherein, the concentration is the effective antifungal concentration in the eye region of mammals; c) ophthalmic adjuvant. The preparation method is characterized in that the composition is changed together with at least one liquid or semi-liquid carrier or adjuvant into an applicable ophthalmic medicament form. The usage of the composition is that ophthalmic preparation which is used for treating and preventing the concurrent infection of bacterium and fungi in the eye region is prepared. The medicinal composition of the invention is capable of playing an antibacterial and antifungal role and avoiding untoward effect such as contraindication, irritation and allergy caused by unilateral medication.
CN101863850A Method for separating epigoitrin and S-goitrin in (R, S)-goitrin The invention provides a preparation method of epigoitrin and S-goitrin which is an antipode of the epigoitrin. The method comprises the following steps of: adding a solvent to (R, S)-goitrin to prepare a solution; carrying out chiral separation by adopting a high efficiency liquid chromatography, wherein normal hexane-isopropanol or normal hexane-ethyl acetate or normal hexane-isopropanol-diethylamine or normal hexane-ethyl acetate-diethylamine is used as a mobile phase, and an ultraviolet detector is used as a detector; and collecting fractions, wherein according to the appearance sequence, the frictions are respectively the optical pure epigoitrin and the S-goitrin. The method has simplicity, high efficiency, high separation degree and high monomer purity.
EP2682005A1 A dietary supplement composition Suggested is a dietary supplement composition comprising one or two anthocyanins, wherein the anthocyanin radical of said anthocyanins are essentially selected from the group consisting of (a) Delphinidin and/or (b) Cyanidin, and the corresponding sugar radicals are essentially selected from the group consisting of glucose, galactose, xylose, arabinose, rutinose, sophorose, sambubiose, or their mixtures, wherein (i) the content of disaccharides is less than about 2 % b.w. and (ii) optionally the content of potassium is about 10 to 5.000 ppm - both calculated on the composition.
CN102018660A Naftopidil suppository and preparation method thereof The invention relates to naftopidil suppository and a preparation method thereof. The naftopidil suppository comprises the following components in part by weight: 10 to 25 parts of naftopidil, 10 to 60 parts of oleaginous substrate, 10 to 60 parts of water-soluble substrate, 1 to 10 parts of surfactant, 10 to 30 parts of hardening agent and 5 to 15 parts of absorbefacient. The suppository is uniformly dispersed, has high dissolution rate and improves the bioavailability and the effectiveness of medicaments.
EP1666067A1 Drug containing chymase inhibitor as the active ingredient The present invention provides drugs containing chymase inhibitors as active ingredients for improving glucose intolerance or preventing and/or treating diseases caused by glucose intolerance. The diseases caused by glucose intolerance are diabetes and/or diabetes complications, wherein the diabetes complications include diabetic nephropathy, diabetic retinopathy, diabetic peripheral neuropathy, hyperinsulinism, insulin resistance syndrome, arteriosclerosis, acute coronary syndrome, arteriosclerosis obliterans, angitis, stroke, hypertension, renal insufficiency, nephropathy, nephritis, renal artery aneurysm, renal infarction, obesity and the like.
CN102190632A 2,4,5-trisubstituted selenazole compounds and preparation method, compositions and application thereof The invention relates to 2,4,5-trisubstituted selenazole compounds and a preparation method, a composition and application thereof, in particular to compounds in a formula (I), or all possible isomers, predrugs, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein each substituent is shown as the description. The invention also relates to a method for preparing the compounds in the formula (I), medicinal compositions comprising the compounds in the formula (I), and application of the compounds in the formula (I) or the medicinal compositions in preparation of medicines for treating and/or preventing phospholipid transfer protein (PLTP) activity increase and/or diseases or syndromes related with the phospholipid transfer protein activity increase. The compounds in the formula (I) have good effect of inhibiting the PLTP activity and/or cholesteryl ester transfer protein (CETP) activity of blood plasma, and can be used for treating diseases on the basis.
EP1608360A1 Synergistic hepatoprotective composition and a method thereof The present invention relates to a synergistic formulation comprising trans-tetracos-15-enoic acid (t-TCA) and andrographolide (AP) in the ratio ranging between 1:7 to 7:1 (w/w), useful in hepatoprotection; and a process for the preparation of a synergistic formulation comprising trans-tetracos-15-enoic acid (t-TCA) and andrographolide (AP) useful in hepatoprotection, said process comprising steps of grounding the particles of the t-TCA and AP into fine particles, mixing the fine particles in ratio ranging between 1:7 to 7:1 (w/w), and grinding the mixture to obtain formulation, and also, a method of hepatoprotection of a subject using the synergistic formulation comprising trans-tetracos-15-enoic acid (t-TCA) and andrographolide (AP), said method comprising the steps of administering the formulation to the subject.
WO2011057437A1 Anti-epidemic growth factor receptor antibody and encoding genes and uses thereof The present invention discloses an anti-epidemic growth factor receptor (EGFR) antibody, genes encoding said antibody, a method for preparing said antibody, inhibitors and medicaments comprising said antibody and/or encoding genes, and uses of said antibody and/or encoding genes for prevention and/or treatment of tumor.
WO2009129510A3 Sulindac formulations in a biodegradable material Effective treatments of pain and/or inflammation for extended periods of time are provided. Through the administration of an effective amount of sulindac or a pharmaceutically acceptable salt thereof at or near a target site, one can relieve pain and/or inflammation caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discongenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days, at least twenty-five days. In some embodiments, the relief can be for at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.
EP2014292A2 Fenoldopam for treatment of acute renal failure The invention relates to the treatment of acute renal failure or acute renal insufficiency in a patient comprising the administration of fenoldopam or an analogue thereof. The medicament can be administered to one renal artery or to both renal arteries.
WO2013152683A1 Bicycle substituted pyrazoloneazo derivatives and preparation method and use thereof The present invention is in the medical and chemical field, and relates to a class of bicycle substituted pyrazoloneazo derivatives, the preparation method and a pharmaceutical composition and use thereof. In particular, the present invention relates to a compound shown as formula (I) and a pharmaceutically acceptable salt and solvate thereof. The present invention also relates to the preparation method of the compound of formula (I), a pharmaceutical composition comprising same and the use thereof in preparing medicine. The compound of formula (I) of the present invention is an effective TPO agonist and a good drug for treating thrombocytopenia.
US20130011496 Cancer testis antigens as biomarkers in non-small cell lung cancer A cancer testis antigen biomarker useful to determine whether a non- small cell lung cancer tumor is likely to respond to neoadjuvant chemotherapy is provided. Methods of using the biomarker in the diagnosis, treatment and prognosis of non-small cell lung cancer also are provided.
CN103230390A Application of salvianolic acid B in preparing medicines used in protection of arsenic-trioxide-induced cardiotoxicity and with synergetic antitumor effect The invention discloses an application of salvianolic acid B in preparing medicines used in protection of arsenic-trioxide-induced cardiotoxicity and with synergetic antitumor effect. The salvianolic acid B in the invention can be salvianolic acid B medicine compositions including various preparations of oral or parenteral administration forms. When the composition is used in oral administration, the composition can be tablets, capsules, soft capsules, oral liquid, syrup, granules, dropping pills, oral disintegrating tablets, sustained-release tablets, sustained-release capsules, controlled-release tablets, and controlled-release capsules. When the composition is used in parenteral administration, the composition can be water injection, lyophilized powder injection, sterile powder injection, and infusion. Tablets and water injection are preferable preparation forms of the medicine composition provided by the invention.
US20100056485 Nanosoap containing silver nanoparticles Disclosed herein is a silver nanoparticle based antimicrobial composition and methods for making the same. The antimicrobial composition comprises an amphiphilic molecule having at least one hydrophilic group and at least hydrophobic groups attached thereto; and an at least one silver nanoparticle in contact with the amphiphilic molecule. Also disclosed are uses for the antimicrobial composition such as for the treatment of skin disorders.
CA2857226A1 Prophylactic compositions for management of microbial infections in patients with brain injury The present disclosure pertains to antimicrobial compositions for intravenous administration to patients who have experienced a serious brain trauma, to reduce the risk of occurrence of post-trauma microbial infections. The antimicrobial compositions comprise an a-galacytosylceramide compound and one or more excipients. The present disclosure also pertains to the use of a-galacytosylceramide compounds for the manufacture of antimicrobial medicaments for intravenous administration to patients with serious brain traumas. The present disclosure also pertains to methods for the prophylactic use of the antimicrobial compositions to reduce the risks of occurrence of post-trauma microbial infections.
US7858105 reducing pigmentation of skin for cosmetic effects by administering tyrosine hydroxylase inhibitors to prevent the biosynthesis of DOPA and catecholamines; thioacetanilide; hyperpigmentation-related medical conditions such as melasma, age spots, freckles, ochronosis, and lentigo Methods and formulations are provided to reduce pigmentation in skin, using an array of compounds selected from benzimidazoles, phenylthioureas, phenylthiols, phenylamines, bi- and multicyclic phenols, thiopheneamines, and benzothiamides. The compounds preferably inhibit pigment synthesis in melanocytes through the tyrosinase pathway. The methods can be used for lightening skin, and for treating uneven skin complexions which result from hyperpigmentation-related medical conditions such as melasma, age spots, freckles, ochronosis, and lentigo. The compounds can be used medically or cosmetically.
EP1033997B1 Method of mobilizing hematopoietic stem cells A method of mobilizing hematopoietic stem cells from the bone marrow to the peripheral circulation is provided by administering to an animal an effective amount of mature, modified or multimeric forms of KC, groβ, groα or groη.
CN101234119A Compound soluble powder for preventing and controlling pig intestinal bacterial disease The invention relates to a compound soluble powder used for preventing and curing bacterial diseases in pig intestinal, which consists of a principle agent and an excipient. The medicine components and weight percentage included in a complete formula are as follows: 3.8 percent of apramycin sulfate, 1.9 percent of doxycycline hydrochloride, 1.5 percent of neomycin sulfate, 0.8 percent of gentamicin and 92 percent of soluble starch. The compound soluble powder of the invention has the following advantages: (1) developing a novel compound preparation for preventing and curing bacterial diseases in pig intestinal in veterinary clinic practice; (2) reasonable composing prescription; the medicine selected is chosen on the basis of in vitro chemosensitivity assay for 1,500 isolated bacteria in intestinal canal in domestic animal and poultry from 23 provinces of China and screened through systemic combined chemosensitivity test; (3) safety, high efficiency, low toxicity, low residue and convenient operation; (4) simple production technique, stable preparation, accurate dosage and controllable quality.
WO2013150295A1 Food supplement to support brain function The present invention relates to a food supplement to support brain function, including cognitive functions such as memory. The food supplement comprises one or more active ingredients selected from the group consisting of uridine, cytidine, glutamine, pantothenic acid, iron, colostrinin and caffeine.
US20120010213 Oral controlled release dosage forms for water soluble drugs Disclosed herein is an oral controlled release pharmaceutical formulation comprising water-soluble drug or pharmaceutically acceptable salts thereof, in a hydrophilic matrix system, further comprising pH independent polymers present in an amount of 5% to 90% w/w in combination with acid insoluble polymer present in an amount of 1% to 70% w/w and/or a diluent, a lubricant and/or a glidant.
CN102772394A Multifunctional antiseptic and detersive medicament for external use The invention discloses a multifunctional antiseptic and detersive medicament for external use, which is prepared by phenol, camphor, borneol and alcohol. The medicament has the functions of regulating vital energy, invigorating circulation of blood, removing stasis, sterilizing and callusing and the like, has significant curative effects for various traumas or postoperative recovery and non-healing wounds, and delayed healing of wounds. The invention also has curative effects of preventing and treating otitis media, skin infection, fire burn, pesticide burn, tumours, cancers, syphilis, traumatic injuries, and various non-healing surgical cuts, and is capable of shortening healing time of the wounds, so that healing periods of various long-term non-healing traumas can be shortened by one fifth; furthermore, long-term clinical observation and treatment prove that the multifunctional antiseptic and detersive medicament is more definite in treatment effect, takes effect more instantly, stronger in stability, less in pain of patients and lower in cost; no sequelae, anaphylaxis and toxic and side effects are produced after healing, so that the patients are easy to accept; and the effective rate reaches up to 99% and the cure rate reaches above 96%.
CN1660082A Microcapsule in multilayer film in use for antifan and preparation method A metindol microsoftgel with multiple film layers for regulating its release speed is prepared through proportionally adding the metindol microcrystals to the acidic aqueous solution of sodium alginate containing inorganic salt, stirring for adsorbing sodium alginate sufficiently, removing excessive sodium alginate, adding the aqueous solution of chitosan containing inorganic salt, stirring for adsorbing chitosan sufficiently, removing excessive chitosan, and alternatively repeating said adsorptions.
US7727992 2-(3-Ethyl-ureido)-6-pyridin-3-yl-3H-benzoimidazole-4-carboxylic acid methyl ester; for treating bacterial infections in mammals; useful in treating or lessening severity of urinary tract infections, pneumonia, prostatitis, skin and soft tissue infections, intra-abdominal infections The present invention relates to compounds which inhibit bacterial gyrase and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to a method for preparing these compounds.
WO2012149358A1 Injectable preformed macroscopic 3-dimensional scaffolds for minimally invasive administration The invention provides polymer compositions for cell and drug delivery.
US20060100180 Composition containing an androgenous 11b-halogen steroid and a progestational hormone, and male contraceptive based on said composition The invention relates to a novel chemical composition containing an androgenous 11β-halogen steroid and the progestational hormone of formula (I), to a pharmaceutical composition containing said chemical composition and to a male contraceptive based on said pharmaceutical composition.
US20120196894 Novel trpa1 antagonists The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.
CN102250064A Glutamic acid derivants The invention relates to glutamic acid derivants and medicinal application thereof. The glutamic acid derivants disclosed by the invention are targeted specific inhibitors generated aiming at tumor necrosis factors and angiogenesis, can be used for treating indications, such as malignant tumor, lepriasis erythema nodosum, septicemia, diabetes mellitus, osteoporosis, multiple sclerosis, rheumatoid arthritis, and the like, and has low using dosage and little side effect.
US20110059091 Inhibitors of oncogenic isoforms and uses thereof Isoform-binding molecules that specifically bind to one or more isoforms expressed and/or associated with oncogenic phenotypes in a hyperproliferative cell (e.g., a cancerous or tumor cell) are disclosed. The isoform-binding molecules can be used to treat, prevent and/or diagnose cancerous conditions and/or disorders. Methods of using the isoform-binding molecules to selectively detect oncogenic isoforms, to reduce the activity and/or induce the killing of a hyperproliferative cell expressing an oncogenic isoform in vitro, ex vivo or in vivo are also disclosed. Diagnostic and/or screening methods and kits for evaluating the function or expression of an oncogenic isoform are also disclosed.
US20110073518 Generally Linear Effervescent Oral Fentanyl Dosage Form and Methods of Administering Fentanyl containing dosage forms and methods using same are described. These dosage forms include substantially less fentanyl by weight than know oral formulation and have advantages in terms of cost and side effects. These dosage forms are intended for oral administration of fentanyl across the oral mucosa.
WO2007080270A3 New cholest-4-en-3-one oxime derivatives, pharmaceutical compositions comprising them, and preparation process Compound of the formula (I) in which X represents an oxygen atom or an =N-OH group and R represents a group selected from (II) or one of its esters and/or its addition salts with pharmaceutically acceptable acids, particularly as a cytoprotective, preferably cardioprotective and/or neuroprotective, medicament; the compounds of formula I in which R is R2, R3, R4, R5 or R6, as new compounds; and also their preparation process, and the use.
CN102949709A External gel used for treating diabetic foot, and preparation method and application thereof The invention relates to an external gel used for treating diabetic foot, and a preparation method and an application thereof. Specifically, the invention relates to an external gel preparation with oxygen-carrying and antibacterial materials, and containing recombinant human epidermal growth factor (rhEGF). The preparation basically comprises: a medicine component recombinant human epidermal growth factor (rhEGF), an oxygen-carrying material, an antibacterial material, a gel substrate, a stabilizing agent, a humectant, a penetration enhancing agent, a surfactant, and a pH regulation agent.
US20110275619 Inhibitors of bace1 and methods for treating alzheimer's disease Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described.
CN101683352A Helminthic for aquaculture of aquatic animal and preparation method thereof The invention relates to a helminthic for the aquaculture of aquatic animals and a preparation method thereof, belonging to the field of aquaculture industry, in particular to an external helminthic acting on zooplanktons of a water body and the aquatic animals. The technical scheme is achieved by the following steps: using a right amount of dimethylbenzene to dissolve 0.2-1.5 parts by weight of ivermectin; then sequentially adding 2-5 parts by weight of glycerol, 2-5 parts by weight of isopropanol and 2-5 parts by weight of tween-80; uniformly stirring; then adding the balance of the dimethylbenzene with the volume defined into 100 parts, and uniformly stirring. The helminthic has better effect on killing cladocera inside the water body of a culture pond and parasites, such as spiny-headed worms, eelworms, dactylogyrus, gyrodactylus, trichodina, and the like which are parasitized on the body surfaces or the gills of the aquatic animals, and better curing effect on various diseases caused by the parasites especially without residues inside bodies of the aquatic animals, enables the production quality of the aquatic animals to accord with the national requirements and ensures the edible safety of the aquatic animals for people.
EP2773339A1 Composition for improving neuropsychological test battery score The invention relates to a composition comprising: (i) one or more of uridine and cytidine, or salts, phosphates, acyl derivatives or esters thereof; and (ii) a lipid fraction comprising at least one of docosahexaenoic acid (22:6; DHA), eicosapentaenoic acid (20:5; EPA) and docosapentaenoic acid (22:5; DPA),or esters thereof, for use in the improvement of the composite NTB score. The invention also provides an improved NTB method comprising an optimized set of individualized tests, in particular for a (prodromal or mild) Alzheimer's or dementia patient.
CN1813730A Fexofenadine hydrochloride dropping pill and its preparing method The present invention discloses a medicine fexofenadine hydrochloride dripping pills preparation for effectively curing seasonal allergic rhinitis and chronic idiopathic urticaria and its preparation process. It is made up by using fexofenadine hydrochloride and matrix for making dripping pills.
CN102631354A Pharmaceutical composition containing vitamin D and metformin The invention provides a pharmaceutical composition containing vitamin D and metformin. Particularly, the invention provides a pharmaceutical composition which comprises an active component (a) of vitamin D; an active component (b) of metformin or its pharmaceutically acceptable salts; and (c) a pharmaceutically acceptable carrier. The pharmaceutical composition of the present invention can prevent and treat colorectal polyps and colorectal cancers synergically, effectively, and safely.
US20120316164 Method for inhibiting the growth of cancer stem cells The present invention provides a method for inhibiting the growth of cancer stem cells, particularly colorectal cancer stem cells, liver cancer stem cells, lung cancer stem cells or breast cancer stem cells, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of antimycin A or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.
WO2014017515A1 4-[5-(pyridine-4-yl)-1h-1,2,4-triazole-3-yl]pyridine-2-carbonitrile crystalline polymorph and production method therefor Provided are a 4-[5-(pyridine-4-yl)-1H-1,2,4-triazole-3-yl]pyridine-2-carbonitrile crystalline polymorph, which is useful as a pharmaceutical product, and a production method therefor. The present invention relates to a 4-[5-(pyridine-4-yl)-1H-1,2,4-triazole-3-yl]pyridine-2-carbonitrile crystalline polymorph, and three different crystalline forms are obtained by purification via a salt, storage under humidified conditions or recrystallization.
CN103648588A Compounds for the treatment of cancers associated with human papillomavirus The present invention relates to the pyrrolidine substituted with flavone derivatives, represented by the compounds of Formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a diastereoisomer thereof for use in the treatment of cancers associated with human papillomavirus. The present invention also relates to the pharmaceutical compositions containing the compounds of Formula (I) for the treatment of cancers associated with human papillomavirus.
US20120064181 P2X3 Receptor Antagonists for Treatment of Pain The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
WO2014146747A1 Piperazine derivatives as fasn inhibitors Compounds of the formula (I), in which R, X1, X2, X3, X4, R1, R2 and q have the meanings indicated in Claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
EP1951692B1 Oxazole and thiazole ppar modulator The invention provides compounds (I) pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPARδ.
US20120142630 Process for purifying guar The present invention relates to processes for purifying guar comprising combining borate and guar in an aqueous solution and treating the aqueous solution with an organic solvent to induce precipitation of purified guar. Another embodiment of the present invention is directed to ophthalmic formulations comprising purified guar produced by the processes described.
CN103083277A Antifungal capsule for dogs and cats The invention discloses an antifungal capsule for dogs and cats. The drug provided in the invention is the capsule prepared by making itraconazole into particles. Nearly 10 years of wide-range application of the drug itraconazole proves its efficacy and safety. With definite curative effects, the drug disclosed in the invention can effectively alleviate the development of dermatomycosis in dogs and cats.
CN103565806A Roflumilast oral preparation and preparation method thereof The invention provides a roflumilast oral preparation and a preparation method thereof. According to the invention, solvent solid dispersion technology is adopted, and the solid oral preparation is prepared by 0.1-50 wt% of roflumilast and 50-99.9 wt% of pharmaceutically acceptable auxiliary materials. Roflumilast tablets with stable and controllable quality can be produced by using common pharmaceutical equipment, which is helpful for vast patients to obtain cheap and good medicine products.
US20120225841 Methods of Making and Using a Ruminant Gas Reduction Composition A method comprising administering an oligosaccharide composition to an organism having a gastrointestinal system to affect the production of GHG produced by the organism allowing for a reduction of the GHG produced by the organism while optimizing the health, feed intake, and protein synthesis of the organism so that management of the organism may realize the synergistic effects of maximizing both typical organism commodity-type concerns (e.g., size and production metrics) and atypical organism commodity-type concerns (e.g., carbon credit trading/monetization). A gas-reducing composition comprising soluble extractable material from a lignocellulosic source. A method of producing a composition, comprising providing a lignocellulosic source; extracting soluble materials from the lignocellulosic source to produce soluble extractable material; and processing the soluble extractable material to yield a gas-reducing composition, wherein the gas-reducing composition comprises hemicellulose and exhibits gas-reducing activity.
EP2155705A2 Compositions for regulating or modulating quorum sensing in bacteria, methods of using the compounds, and methods of regulating or modulating quorum sensing in bacteria The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.
CN102335216A Inhibitor for generation of melanin The invention provides ''an inhibitor for generation of melanin without worry of side effect and advantaged by safety and excellence'', and ''medicines, foodstuff or cosmetic products with melanin generation inhibition'' comprising the inhibitor for generation of melanin. The inhibitor comprises an extract from Saussurea involucrate (Kar.et Kir.) Sch.Blp., the extract uses component isolated from a chromatographic column or dihydro dehydrogenation banksia rose lactone as active ingredients of the inhibitor for generation of melanin, and medicines, foodstuff or cosmetic products with melanin generation inhibition and comprising the inhibitor for generation of melanin.
EP1927591A1 Polymorphic Forms of Deferasirox (ICL670) The invention relates to crystalline forms of 4-[3,5-bis(2-hydroxypheny1)-[1,2,4]triazol-1-yl]benzoic acid and to its amorphous form, to processes for the preparation thereof, to compositions containing the same and their uses for the manufacture of a medicament for the treatment of the human body. Normal text
WO2007124447A2 Use of chalcogenides for treating shock and other adverse conditions The present invention concerns the use of active compounds for inducing apnea and treating shock, in addition to enhancing the survivability of a subject. It includes compositions, methods, articles of manufacture and apparatuses for enhancing survivability and for achieving these effects.
US20120258959 Pyridone gpr119 g protein-coupled receptor agonists Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.
CN1985925A Extraction, application and medicine composition of franchet groundcherry steride The present invention relates to medicine composition, and is especially extraction, application and medicine composition of franchet groundcherry steride. Franchet groundcherry steride is used in treating hyperlipemia and diabetes, with the effective rate reaching 100 %. The extraction process includes decoction, centrifuging, ultrafiltering and concentrating to obtain extractum containing franchet groundcherry steride. The medicine composition of franchet groundcherry steride may be prepared with franchet groundcherry steride in 65-75 wt%, haw flavone in 15-25 wt% and rhubarb in 5-10 wt%; or prepared with franchet groundcherry steride in 55-65 wt%, curcumin in 32-40 wt% and manyprickle acanthopanax root saponin in 3-5 wt%; or prepared with franchet groundcherry steride in 50 wt%, matrine in 30 wt% and bitter gourd saponin in 20 wt%.
WO2008006581A3 Compositions and use thereof for the treatment, co-treatment or prevention of imflammatory disorders The present invention relates to novel compositions comprising hydroxytyrosol and/ or oleuropein (I) and at least one additional component e.g. selected from the group of ligustilide, oleuropein aglycone, magnolol, honokiol, genistein, resveratrol, EGCG, magnolia bark extract, cashew fruit extract and Glycyrrhiza foetida as well as to the use of these compositions as a medicament, in particular as a medicament for the treatment, co-treatment or prevention of inflammatory disorders.
EP2085089A1 Phospholipids Containing omega-3-Fatty Acids for the Treatment of Overweight, Obesity and Addictive Behavior The invention relates to the use of phospholipids containing ω-3-fatty acids and/or containing low amounts of ω-6 fatty acids, notably phospholipids of marine origin, for the treatment of overweight, obesity and addictive behavior.
CA2517371C Method for the production of flavonoid-containing compositions and their use The present invention relates to a method for the production of plant extracts having a standardized flavonoid content, in particular having a standardized luteolin content. Plant material of Reseda plants which has been pre-extracted with water is extracted with a solvent and then concentrated. The compositions thus obtained are suitable as pharmaceutical or cosmetic products and as colorants. The invention furthermore relates to the use of Reseda extracts for treating skin diseases.
EP1633359A1 Use of efletirizine for treating persistent allergic rhinitis The present invention relates to a pharmaceutical use of efletirizine for the treatment of persistent allergic rhinitis.
CN101194903B Dropping pills containing Isocarboxazid and method for preparing the same The invention provides an isocarboxazid dripping pill and a process for preparation. The invention overcomes the shortcomings of the prior dripping pills that pure natural degrees of findings which are used by the prior dripping pills are not high, and chemosynthesis findings which are commonly used are not in food additives catalogs of some countries, and tastes of the dripping pills are worse. The invention is a pharmaceutical preparation whose natural degree is higher, safety is stronger, and side effect is lower. The medicament is mainly used to depressive patients who are resistant to tricyclic antidepressants. The invention is effective on depression with anxiety and hysteria.
EP2643299A1 Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions The present invention relates to novel bipyridine sulfonamide derivatives of formula (I) and their use for the treatment and/or prophylaxis of a neurodegenerative disease or condition, particularly Alzheimers disease (AD), a cardiovascular disease or a pathology involving ischemia.. Additionally, processes for preparing such derivatives5 and pharmaceutical compositions comprising them are provided.
EP2527008A2 Anticancerous polymeric agents Methods and pharmaceutical compositions for treating cancer, particularly MDR cancer, which utilize polymeric compounds that are composed of a plurality of amino acid residues and one or more hydrophobic moieties are disclosed.
CN101836973A New application of amide compound The invention discloses new application of an amide compound. The amide compound is a compound expressed by a formula I, pharmaceutically acceptable salt thereof or a medicament precursor thereof. The compound is used for preparing a liver cell apoptosis inhibitor.
CN102600195A Composite transdermal linimentum for pets as well as preparation method and application of composite transdermal linimentum The invention discloses a composite transdermal linimentum for pets as well as a preparation method and an application of the composite transdermal linimentum. The composite transdermal linimentum consists of 0.1 to 0.5 part of ivermectin, 0.5 to 1.5 parts of metronidazole, 5 to 15 parts of azone, 10 to 30 parts of glycerin methylal and 150 to 250 parts of propylene glycol, wherein the unit of the ivermectin and the metronidazole is the weight unit of g, and the unit of the azone, the glycerin methylal and the propylene glycol is the volume unit of mL. The preparation method of the composite transdermal linimentum comprises the following steps that: the glycerin methylal and partial propylene glycol are uniformly mixed and preheated, then, the ivermectin and the metronidazole are added, after the complete dissolution, the azone and the rest propylene glycol are added and are uniformly stirred, and the composite transdermal linimentum is obtained. The invention widens the preparation types of the ivermectin in clinics for veterinarian, in addition, the ivermectin is reasonably matched with anti-anaerobe medicine of metronidazole, the curative effect of the prepared composite transdermal linimentum is obviously superior to that the existing single ivermectin medicament, in addition, the irritation and the toxicity are low, the stability is high, the composite transdermal linimentum can be used as a critical disease medicament for pets, and good practical values are realized.
EP1734946B1 Punicic acid for use to enhance immune response and treating inflammatory bowel disease Disclosed is a method of enhancing the immune response of an animal, including mammals and humans, to prevent or ameliorate immunoinflammatory diseases such as Inflammatory Bowel Disease, increase immune system development, maintain or increase CD4+ and CD8+ T lymphocyte levels, increase immune function, increase immune response against viruses and prevent or ameliorate the Metabolic Syndrome, Type 2 diabetes and obesity by administering orally or parentally a therapeutically effective amount of punicic acid to the animal.
CN101869711A Medicament composition containing diuretic antihypertensive medicament and biguanide antidiabetic medicament and applications thereof The invention relates to a medicament composition containing diuretic antihypertensive medicament, biguanide antidiabetic medicament and a pharmaceutically acceptable carrier. The invention also relates to the applications of the composition in the preparation of medicaments for preventing or treating diabetes mellitus with hypertension. The implementation of the invention provides the medicament composition with specific applications, and the medicament composition not only has a precise curative effect, but also can improve the compliance of patients. The patients can take the medicament conveniently, and the medical expense is reduced. The invention has a better market prospect, and belongs to the field of pharmacy.
CN103239394A Small-volume moxifloxacin hydrochloride injection and preparation method thereof The invention relates to a small-volume moxifloxacin hydrochloride injection and a preparation method thereof. The preparation method comprises the following steps of: regulating the PH value of 0.01-0.04/ml of moxifloxacin hydrochloride water solution for injection to 4.2-4.7, adding activated carbon for absorption, treating by a filter membrane of 0.22mu m, filling nitrogen, encapsulating and sterilizing to prepare 10ml of small-volume injection. The injection product does not have sub-visible particles, is good in clarity and safe in medication, can be conveniently mixed with injections such as glucose, mannitol and the like, and is not restricted to a sodium chloride injection. The invention solves the problem that the sodium chloride injection can not be used for some patients having specific physiques.
CN101948458A Baicalein derivatives with antitumor activity and application thereof in medicines The invention relates to the field of medical chemistry, in particular to flavonoids (I) of baicalein derivatives. The definitions of R5, R6, R7 and X in the formula refer to the specification. Pharmacological tests prove that the flavonoids have obvious antitumor activity.
CN102827039A Herba Houttuyniae derivative and its application in drugs The invention relates to a Herba Houttuyniae derivative, or its ester, enantiomer, diastereomer, stereomer, tautomer, hydrate, solvate, prodrug or pharmaceutically acceptable salt, a preparation method of the Herba Houttuyniae derivative and an application of the Herba Houttuyniae derivative in drugs, and also relates to a drug composition of the above compounds, and uses of the compounds and the drug compositions in the preparation of antibacterial and antiviral drugs. The compounds and the drug composition are especially suitable for treating a plurality of urinary system diseases, and have the advantages of good water solubility, high biological utilization degree, and high purity, so toxic side effects and stimulation effects caused by low purity are substantially reduced.
US20070060582 1,4-Disubstituted isoquinilone derivatives as raf-kinase inhibitors useful for the treatment of proliferative diseases This invention relates to compounds of the formula (I) wherein the variable substituents are described herein. The compounds are useful for the treatment of conditions and diseases characterized by an aberrant MAP kinase signaling pathway, such as cancer.
WO2013096785A1 2-substituted-thienoquinolones and related compounds as anti-infective agents Disclosed herein are 2-substituted-thienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R3, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a 2-substituted-thienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a 2-substituted-thienoquinolone to an animal suffering from a microbial infection.
CN103113335A Benzoquinone compound and use thereof for preparing anti-tumour drug The invention belongs to the field of pharmacy and relates to a benzoquinone compound and use thereof for preparing an anti-tumour drug, in particular to preparation of Arnebinone B and use thereof for resisting lung cancer, prostatic cancer and nasopharynx cancer. The benzoquinone compound provided by the invention is Arnebinone B, which is separated from arnebiae. In-vitro anti-tumour activity experimental results show that the median inhibitory concentration of Arnebinone B on lung carcinoma cell A549 is 4.86 mu g/ml, the median inhibitory concentration of Arnebinone B on prostate cancer cell DU145 is 5.16 mu g/ml, the median inhibitory concentration of Arnebinone B on nasopharyngeal carcinoma cell KB is 5.2 mu g/ml, and the median inhibitory concentration of Arnebinone B on KB drug-resistant strain KB-VIN is 4.98 mu g/ml. The result shows that Arnebinone B can be used for preparing the anti-tumour drug, in particular drugs for treating lung cancer, prostatic cancer and nasopharynx cancer.
CN102068448A Application of icariside II in preparation of anti-melanoma medicament The invention belongs to the field of medicament preparation, relates to new medicinal application of icariside II, and particularly relates to application of icariside II in preparation of an anti-melanoma medicament. The icariside II is adopted for intervention experiments of mouse melanoma cell strains and human melanoma cell strains; by observing the inhibiting condition of the icariside II on cell proliferation, the results show that the icariside II can remarkably inhibit the proliferation of B16, A375 and SK-MEL-2 cells in vitro, obviously promote apoptosis of the cells and increase P53 protein phosphorylation and caspace protein expression; and the icariside II can remarkably inhibit loaded B16 mouse subcutaneous transplant tumor volume. Experiment results prove that the icariside II can effectively inhibit the melanoma. The icariside II can further be used for preparing the anti-melanoma medicament by adding proper pharmaceutically-acceptable carriers.
EP0957921B1 17alpha-dihydroequilenin for preventing neurodegeneration and cognitive dysfunction A method of using a steroidal compound, 17 alpha -dihydroequilenin, to prevent and treat neurodegeneration and cognitive dysfunction in estrogen deficient females and to reduce the risk of Alzheimer's related dementia and other senile dementia related conditions in both males and females. The method comprises administering 17 alpha -dihydroequilenin in a therapeutically effective amount to a mammal in need of increased cognitive function or to a mammal susceptible to estrogen deficiency-related neurodegeneration or to senile dementia of the Alzheimer's type.
CN102225937B Antineoplastic alkaloid compound, and its medicine composition, preparation method and application The invention provides vobasine-iboga type alkaloid compound ervachinines A-D (1-4) with antineoplastic activities, its preparation method, a medicine composition containing the alkaloid compound, and an application of the alkaloid compound and the medicine composition in preparation of antineoplastic drugs, wherein structural formulas of the vobasine-iboga type alkaloid compound ervachinines A-Dare shown as the formulas of 1 to 4.
CN102058544B Method for preparing enteric slow release pellet containing fenofibric acid choline salt The invention relates to an enteric slow release pellet containing an active pharmaceutical ingredient of fenofibric acid choline salt, which is characterized by comprising a pill core, an isolation coat layer and a film coat layer for controlling medicament release; and the purpose of medicament enteric slow release can be achieved without additional enteric coat layers. The pill core is prepared by mainly utilizing an extrusion-spheronization method, the coating is carried out by utilizing a fluidized bed.
CN102641306A Anti-heat stress composition for pigs The invention discloses an anti-heat stress composition for pigs. The invention provides the anti-heat stress composition for pigs, wherein 1kg of the composition comprises 15 to 60g of L-ascorbic acid, 10 to 40g of DL-alpha tocopheryl acetate, 10 to 40g of yeast selenium, 0.05 to 0.2g of chromium picolinate and 859.8 to 964.95g of carriers. The composition belongs to the anti-heat stress composition for pigs, the normal life activities of the pigs can be maintained in high-temperature seasons, the anti-stress capability and the disease resistance capability are enhanced, the growth speed is accelerated, the feed consumption is reduced, the death rate is reduced, and the economic benefits of raisers are improved. The composition does not have toxic or side effects and does not have adverse influence on the environment.
CN103356541A Application of Sarcaboside B in medicine used for treating gastric cancer The invention discloses an application of Sarcaboside B in preparation of a medicine used for treating gastric cancer and belongs to the technical field of new applications of medicines. In vitro MTT (methyl thiazolyl tetrazolium) antineoplastic activity evaluation shows that Sarcaboside B has an obvious inhibitory effect on growth of human gastric cancer cell strains HGC-27, MGC-803, BGC-823 and SGC-7901, so that Sarcaboside B can be used for preparing an anti-gastric-cancer medicine and has a good development application prospect; the application of Sarcaboside B in preparation of the medicine used for treating gastric cancer is disclosed for the first time, a brand new skeleton type is adopted, and Sarcaboside B has an unexpected inhibitory activity on gastric cancer cells.
US7803791 biological conjugate drug comprising enzyme inhibitor antibiotics and protein, for the treatment and/or prophylaxis of bacterial inflammatory processes, solid tumor; norfloxacin with albumin; antiinflammatory agents, antitumor agents The present invention is directed to a Gyrase inhibitor-protein conjugate; in particular a Gyrase inhibitor-albumin conjugate. The present invention further provides methods of the treatment of inflammatory conditions and tumors. Methods of making and producing a Gyrase inhibitor-protein conjugate are also disclosed.
US20080279952 Controlling particle size; overcoating particles; pain therapy eith postoperative or tumor pain; central nervous system disorders; antiepileptic agents; Parkinson's disease; longQT syndrome; potassium channel moderators; muscular disorders; prion disease; Alzheimer's disease; tinnitus ; overactive bladde The present invention relates to compositions and compacts comprising flupirtine or a pharmaceutically acceptable salt thereof in which there is controlled-release of at least a portion of flupirtine or a pharmaceutically acceptable salt thereof. The invention further relates to kits comprising such compositions and compacts, and methods of making and using such compositions and compacts.
CN1733073A Analgesic enema liquid for children and its preparation method The invention discloses an analgesic enema liquid for children and its preparation method, which is prepared from baicalin, an extract of scutellaria root 20-500 parts, honeysuckle flower extract (calculated by chlorogenic acid) 5-250, algopyrin 2-600, cellulose 0-1000, starches 0-1000.
US20100143382 Modulation of rhamm (cd168) for selective adipose tissue development Herein is described the methods and compositions for modulation of Rhamm, also known as CD 186, and its effects on wound repair, muscle differentiation, bone density and adipogeneisis through its ability to regulate mesenchymal stem cell differentiation. Compositions and methods are provided for blocking Rhamm function for selectively increasing subcutaneous, but not, visceral fat. Compositions and methods for modulating Rhamm in wound repair are also described.
CN101897911A Preparation for treating gonorrhea The invention discloses a method for preparing a preparation for treating gonorrhea. The method is implemented by the technical scheme which comprises the following steps of: uniformly spraying crystal sugar on polygonum aviculare, plantain seed, talc, bamboo leaves, rush, alismatis rhizoma and dianthus superbus and uniformly mixing and then spraying the talc on the mixture to steam for 10min; decocting the obtained product in river water in an earthen pot for 20min, wherein the ratio of the obtained product to river water is 1:1; and taking the mixture out and removing residues to obtain a finished preparation. The disease can be cured by the method within three days.
EP2588610A1 Calpain-3 inhibitors for treating muscular dystrophies and cardiomyopathies The present invention relates to a composition comprising a calpain-3 inhibitor for treating cardiomyopathies and muscular dystrophies, in particular tibial muscular dystrophy (TMD).
US20100009929 Compositions including triciribine and bortezomib and derivatives thereof and methods of use thereof This application relates to combination therapies including triciribine and related compounds and bortezomib and derivatives thereof analogs and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
WO2007076460A3 Substituted thiazole ureas useful as inhibitors of protein kinases The present invention relates to compounds and methods useful as inhibitors of protein kinases, including B-Raf and several receptor tyrosine and cytoplasmic tyrosine kinases. The present invention is directed to new substituted pyrimidinyloxy urea compounds of Formula (I) and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulating of protein kinase activity in a human or animal subject are also provided for the treatment diseases such as cancers.
WO2007068171A1 CRYSTALLINE FORM I OF 3,4',5-TRIHYDROXY-STIBENE-3-β-D-GLUCOSIDE The present invention relates to a new crystalline form of 3,4',5-trihydroxy-stilbene-3-β-D-glucoside, its preparation method and the use, as well as a pharmaceutical composition containing the same. The form I of 3,4',5-trihydroxy-stilbene-3-β-D-glucoside of the present invention possesses stable shape and definitive melting point, and has good chemical stability. This new morphology of 3,4',5-trihydroxy-stilbene-3-β-D-glucoside has desired property for preparing solid preparation. When it is prepared in formulation, it has good compacting properties for easy molding, so as to make material cost greatly reduce in industrially pharmaceutical preparation. It is convenient to storage, easy to manufacture operate, and even more tractable for quality control.
US20050124647 For example, 4-hydroxy-1,1-di-(5',6'-methylendioxy-indol-2-yl)-butane; antitumor agents, particularly for treating mammary carcinoma and colon carcinoma Compounds of the formula useful for treating tumors, particularly mammary carcinoma and colon carcinoma.
US7335756 Isolated nucleic acid comprising polynucleotide of given sequence; diagnostic kits; use in treatment of cancer The present invention provides a novel retinoic acid metabolizing cytochrome P450, P450RAI-3, that is predominantly expressed in the adrenal gland. Methods for and uses of the new polynucleotide, polypeptide, fragments thereof and modulators thereof, include the treatment of cancer.
CN102335126A Ornidazole injection and its preparation method The invention relates to a compound pharmaceutical preparation, i.e. an Ornidazole injection and its preparation method. The preparation contains Ornidazole, glacial acetic acid and injection water. The preparation method comprises the steps of: taking a proper amount of injection water (25DEG C-35DEG C), glacial acetic acid and Ornidazole, adding Ornidazole into water and stirring well, adding glacial acetic acid till complete dissolution, adjusting pH to 2.5-4.0, adding activated carbon which is 0.05% (g/ml) of the total volume of the solution, stirring the solution for 15min and conducting filtration, adding water to full capacity (with the temperature of the medical solution controlled between 25DEG C to 35DEG C), then carrying out filtration, embedding, disinfection, light inspection and packaging, thus obtaining the injection. The injection and its preparation method provided in the invention have the characteristics of simple prescription and process, high production efficiency, strong stability of the medical solution, etc.
US20100234371 Bicyclic heterocycles, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof The invention relates to bicyclic heterocycles of general formula (I), in which Ra, Rb, Rc, Rd, Re and X are as defined in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, in particular, the physiologically-acceptable salts thereof with inorganic and organic acids with useful pharmacological properties, in particular, an inhibitory effect on signal transduction brought about by tyrosine kinases, the use thereof for the treatment of diseases, in particular of tumour diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and airways and production thereof.
CN101889986A Flunarizine orally disintegrating tablet and preparation method thereof The invention provides a flunarizine orally disintegrating tablet, which consists of flunarizine and pharmaceutic adjuvant, wherein the pharmaceutic adjuvant comprises a filler, a disintegrating agent, a flavoring agent, an effervescing agent, a lubricating agent and the like. Compared with the disintegrating time limit of a common flunarizine tablet, the flunarizine orally disintegrating tablet has the characteristic of quick response. Mouthfeel observation experiments show that the flunarizine orally disintegrating tablet has good mouthfeel and is easy to be accepted by the patient. In vitro dissolution experiment results show that the bioavailability of the flunarizine orally disintegrating tablet is obviously higher than that of the common flunarizine tablet. The flunarizine orally disintegrating tablet can be quickly dispersed without water or swallow action, and has the advantages of no sand feel, good patient compliance, quick response, and high bioavailability; meanwhile, the preparation process is simple and suitable for industrial production.
CN102319248A Liver cancer resisting micro-molecular compound targeted at mir-122 The invention relates to a novel liver cancer resisting micro-molecular lead compound targeted at inhibiting mir-122. The compound is synthesized on a virtual medicine screening platform based on a combination of bioinformatics and computer technologies. The micro-molecular compound has advantages of good permeability, small toxic and side-effect, simple structure, and easy synthesis. The micro-molecular compound can be used in combination with the tumor necrosis factor (TNF-alpha) for improving the liver cancer killing effect of TNF-alpha. Therefore, liver cancer can be treated. Thus, the compound has potential to be developed into a novel liver cancer resisting medicine.
CN102038700B Bitter-taste-masking erythromycin-cydocarbonate-containing oral composition The invention relates to the field of medicinal preparations, in particular to a bitter-taste-masking erythromycin-cydocarbonate-containing oral preparation and a preparation method thereof. The bitter-taste-masking erythromycin-cydocarbonate-containing oral preparation is characterized by mainly comprising 1 part of erythromycin cydocarbonate, 0.1 to 0.4 part of high-sweetness sugar, 1.0 to 1.5 parts of suspending agent, 5 to 15 parts of filling agent, 0.5 to 2.0 parts of absorbent and 0.1 to 0.2 part of surfactant. The bitter-taste-masking erythromycin-cydocarbonate-containing oral preparation has good mouthfeel, is taken after being mixed with water and improves the compliance of a patient.
CN101978947A Long-acting Cefquinome sulfate injection and preparation method thereof The invention discloses long-acting Cefquinome sulfate injection, which comprises the following component in mass-volume (g/L) part: 25 to 70 parts of Cefquinome sulfate, 2 to 15 part of phospholipid, 2 to 15 part of sorbitan fatty acid ester, 0.1 to 1 part of vitamin E, 0.1 to 0.5 part of vitamin A and the balance of solvent, wherein the solvent is soybean oil for injection. The injection prepared by the invention has long-lasting medicament effect and can achieve an effect, which used to be achieved by the conventional preparations of the same kind through many times of separated injection, through one time of injection, so operation times are reduce, labor and time are saved, stress is reduced and the preparation method is simple in operation.
US7148231 [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride polymorph The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. The [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride is an inhibitor of tyrosine kinase enzymes, and are useful in the treatment of cancer. Also disclosed are methods of making and using the novel polymorph, as well as pharmaceutical compositions containing the novel polymorph.
WO2012130160A1 Aminopyridine derivatives containing acridine ring and use thereof Provided are aminopyridine derivatives containing acridine ring, particularly compounds represented by formula I or formula II, preparation method thereof and use thereof in the preparation of a medicament for inhibiting excessive cell proliferation. Also disclosed are compositions comprising the compounds according to the present invention. The compounds can be used for treating hyperproliferative diseases such as cancers, neuropathic pain, inflammations and the like.
WO2012149452A1 Compounds, formulations, and methods of protein kinase c inhibition The invention provides a method of inhibiting atypical protein kinase C (aPKC) comprising contacting an aPKC with a compound having a structure selected from the group consisting of structural formulas (I) to (IX). The invention further provides a method of inhibiting or reducing vascular permeability. The method comprising administering to a subject a composition comprising an amount of a compound having a structure selected from the group consisting of structural formulas (I) to (IX) effective to inhibit or reduce vascular permeability. A method of treating or preventing a disease or disorder characterized by abnormal vascular permeability, a method of inhibiting angiogenesis, a method of inhibiting cancer cell proliferation, a formulation, and a method of preparing a formulation also are provided.
CN101141956B Use of CRTH2 antagonist compounds in therapy,its preparation method and pharmaceutical uses The invention relates to compounds of general formula (I) wherein R<1>, R<2> , R<3> and R<4> are independently hydrogen, halo,C1-C6 alkyl, -O(C1-C6 alkyl), -CON(R<11>)2 , -SO<11>, -SO2R<11>, -SO2N(R<11>)2, -N(R<11>)2, -NR<11>COR<11>, -CO2R<11>, -COR<11>, -SR<11>, -OH, -NO2 or -CN; each R<11> is independently hydrogen or C1-C6 alkyl; R<5> and R<6> are each independently hydrogen, or C1-C6 alkyl or together with the carbon atom to which they are attached form a C3-C7 cycloalkyl group; R<7> is hydrogen or C1-C6 alkyl; R<8> is an aromatic moiety optionally substituted with one or more substituents selected from halo, C1-C6 alkyl, -O(C1-C6)alkyl, -CON(R<11>)2, -SOR<11>, -SO2R<11>, -SO2N(R<11>)2, -N(R<11>)2, -NR<11>COR<11>, -CO2R<11>, -COR<11>, -SR<11>, -OH, -NO2 or -CN; wherein R<11> is as defined above; R<9> is hydrogen, or C1-C6 alkyl; provided that: R<8> is not phenyl substituted with -COOH; when any two of R<1>, R<2> , R<3> and R<4 >are hydrogen, neither of the other two of R<1>, R<2> , R<3> and R<4> is C3-C6 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs useful in the preparation of pharmaceuticals for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
WO2008111497A1 Prophylactic or therapeutic agent for ophthalmic disease associated with oxidative stress, comprising triterpenoid as active ingredient Disclosed is a novel prophylactic or therapeutic agent for an ophthalmic disease associated with oxidative stress. A compound represented by the general formula (I) or a salt thereof has an excellent activity of inducing the phase-II enzyme in the xenobiotic metabolism system in a posterior ocular tissue such as a neuroretina, a retinal pigment epithelium and a retina/choroid, and is therefore useful as a prophylactic or therapeutic agent for an ophthalmic disease associated with oxidative stress, such as age-related macular degeneration, diabetic retinopathy, diabetic macular edema, retinitis pigmentosa, proliferative vitreoretinopathy, retinal embolism, retinal vein occlusion, uveitis, Lever's disease, retinopathy of prematurity, retinal detachment, retinal pigment epithelial detachment, an optic neuropathy induced by any one of these diseases, an optic neuropathy induced by glaucoma, an ischemic optic neuropathy, and cataract. (I)
WO2013111077A1 Pharmaceutical composition as a substance for antireflux antacid drug Pharmaceutical composition comprising sodium alginate, calcium carbonate, potassium bicarbonate, magnesium containing compound and hydroxyapatite for the treatment of acid-dependent diseases of the gastrointestinal tract.
CN101264092A Compound preparations with ciclesonide and formoterol as active component and preparation and application thereof The invention relates to a compound preparation which takes ciclesonide and formoterol as the active components. The invention also relates to a preparation method and a use of the compound preparation. The invention takes the ciclesonide and formoterol as the medicinal active components and forms a medicinal composition with acceptable accessories in pharmacy. The formulations supplying through mouth, such as dry powder inhaler and aerosol prepared according to the technical means of the invention, have the advantages of rapid effect, quick action and convenient use. The compound preparation can be used for curing different classes of asthma.
US20110288084 [4-( 1-amino-ethyl) - cyclohexyl ] - methyl - amines as antibacterials The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation.
WO2014082737A1 Specific carboxamides as kcnq2/3 modulators The invention relates to specific carboxamides of formula (I) as KCNQ2/3 modulators, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
US20080070968 1-(4-fluoro-phenyl)-8-(4-methyl-benzyl)-1,4,5,6,7,8-hexahydro-cycloheptapyrazole-3-carboxylic acid (1,3,3-trimethyl-bicyclo[2.2.1]hept-2-yl)-amide; antidepressant, anxiolytic; nervous system disorders, metabolic disorders, obesity This invention is directed to a hexahydro-cycloheptapyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
CN101830879A 5-phenoxybutyldimethylapiolin, preparation method and application The invention relates to a method for preparing 5-phenoxybutyldimethylapiolin (5PB-DMA). The method comprises the following steps of: (1) dissolving apiolin (API) in an aprotic solvent and adding dimethyl sulfate (Me2SO4) and anhydrous potassium carbonate (K2CO3) at a certain temperature; continuously stirring and reacting for several hours and then stopping reacting to obtain a reaction product; decompressing to evaporate off the solvent and drying to obtain dimethylapiolin (DMA); and (2) dissolving the DMA into another aprotic solvent and adding 4-phenoxy bromobutane (4-PBB) and the anhydrous potassium carbonate (K2CO3); reacting for several hours and then stopping reacting to obtain a reaction product; decompressing to evaporate off the solvent and dissolving an obtained solid product into water; then filtering and dissolving an obtained solid part into absolute alcohol; and recrystallizing, filtering and drying to obtain the product 5-phenoxybutyldimethylapiolin (5PB-DMA). The method has the characteristics of low cost, high yield, simple and convenient operation, moderate condition, high product purity, environmental protection, and the like and is suitable for industrial production.
US20090318564 Process for preparing and drying solid rasagiline base Disclosed is crystalline R(+)-N-propargyl-l-aminoindan containing water at an amount of less than 0.5% by weight and a pharmaceutical composition comprising the same, and the process for the manufacture and the validation thereof. Also disclosed is a process for the preparation of solid rasagiline base.
US20060004044 3-glyoxylamideindoles for treating cancer Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by Structural Formula (I) (preferably an effective amount). Also disclosed is a method of treating a subject with cancer by administering to the subject an effective amount of a compound represented by Structural Formula (I).
US7192950 Psychological disorders; eating disorders; dietetics The invention relates to novel benzazepines and related heterocyclic derivatives (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
WO2008029266A1 Stearoyl coa desaturase inhibitors The present invention relates to novel Stearoyl CoA desaturase (SCD) inhibitors and uses thereof for treating diseases, conditions and/or disorders modulated by a Stearoyl CoA desaturase enzyme. The SCD inihibitors have the formula (I) or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable ester thereof, a tautomer thereof, a regioisomer thereof, a stereoisomer thereof, a enantiomer thereof, a diastereomer thereof, a polymorph thereof, or a pharmaceutically acceptable solvate thereof, wherein the variables are as described herein.
US8003799 Picolinic acid derivatives and their use as fungicides Compounds of general formula (I): in which n, G, Q1, Q2, X1, X2, Y and Z are as defined in the description, process for preparing these compounds, fungicidal compositions comprising these compounds, processes for treating plants by applying these compounds or compositions.
CN101904843A Compound for preparing bone destruction inhibitor The invention relates to application of a compound with a structural formula I in preparing a mammal bone destruction inhibitor. The medicament can be prepared into formulations for oral administration, such as tablets, capsules, powder, particles, crystals, solution, suspension, decoction, syrup, elixir, tea and masticatories, and can also be prepared into transdermal formulations or formulations for topical administration, such as suspension, gel, ointment, cream, emulsion and powder. The structural formula I is shown in the description.
CN102697751A Enrofloxacin effervescent dispersible tablets special for animals and preparation method of same The invention belongs to the field of pharmaceutical preparation, and discloses enrofloxacin effervescent dispersible tablets special for animals and a preparation method of same. The enrofloxacin effervescent dispersible tablets are prepared from the following components in part by weight: 5 to 20 parts of enrofloxacin hydrochloride raw material, 10 to 35 parts of alkaline effervescing agent, 5 to 25 parts of acid effervescing agent, 1 to 3 parts of adhesive, 78.98 to 116.9 parts of filling agent, and 0.02 to 0.1 part of flavoring agent. The enrofloxacin effervescent dispersible tablets prepared by the method have the advantages of convenience in carrying and transportation and high biological availability, and can generate a large number of bubbles in water and also can be dissolved in a short time so as to achieve the characteristics of fast effect and high biological availability. Furthermore, the enrofloxacin effervescent dispersible tablets prepared by the method can generate a large amount of carbon dioxide when being fast dissolved in water, so that the solution becomes acid and can paralyze taste bud to achieve the flavoring effect, and the bitter and astringent taste of the medicament can be improved. Meanwhile, the effervescent dispersible tablets can be directly used without being weighed and are used for disease treatment for an individual farmer or group farmers.
WO2011114148A1 4h- [1, 2, 4] triazolo [5, 1 -b] pyrimidin-7 -one derivatives as ccr2b receptor antagonists The present invention relates to novel compounds for use in the compositions, to processes for their preparation, to intermediates useful in their preparation and to their use as therapeutic agents. The present invention also relates to pharmaceutical compositions, which comprise compounds that act via antagonism of the CCR2b receptor for which MCP-1 is one of the known ligands and so may be used to treat inflammatory disease, atherosclerosis, diabetes, obesity, cancer, chronic obstructive pulmonary disease (COPD) rheumatoid arthritis and/or neuropathic pain, which is mediated by these receptors.
US20120148506 Antiseptic pharmaceutical composition for oral hygiene and the treatment of oral diseases of microbial origin A polyantiseptic antimicrobial pharmaceutical composition for oral use, for the hygiene and treatment of oral diseases of bacterial, mycotic or viral etiology, for over-the-counter sale, without contraindications. The composition does not contain phenolic or, chlorophenolic compounds, and consists of a mixture of hydrogen peroxide, eugenol, natural camphor, zinc sulphate, sodium fluoride, xylitol, cetylpyridinium chloride and excipients. The formulation is used to deodorise, disinfect, astringe and soothe inflammation of the oral area, avoids the neoformation of bacterial plaque, prevents tooth cavities, inhibits the formation of dental tartar, improves the resistance of teeth to cavities, and treats and prevents oral aphthous ulcers.
CN101797253B Bergenin and cetirizine dihydrochloride compound oral administration preparation The invention discloses a compound oral administration preparation containing bergenin\cetirizine dihydrochloride, in particular to a gastric stasis floating type slow-release tablet, which mainly consists of a fast-release coating layer containing the cetirizine dihydrochloride and a slow-release tablet core layer containing the bergenin. The invention further realizes the fast release of the cetirizine dihydrochloride and the gastric stasis and the slow release of the bergenin, and improves the curative effect of the bergenin\cetirizine dihydrochloride compound oral administration preparation. Pharmacodynamic experiments prove that the medicine composition has the obvious effects of relieving the cough, eliminating the phlegm and preventing the asthma, has small side effect, and can be used for treating chronic bronchitis and bronchial asthma.
US20080287526 Pharmaceuticals for treating or preventing oral diseases The present invention discloses a new compound of formula (I), a method of extracting the new compound, as well as various uses of the new compound in manufacturing antibacterial medicaments or oral care products or for other antibacterial uses.
US20070225727 Transparent Tissue-Visualizng Preparation Described is a highly safe means to improve visibility of transparent tissues of the eye, i.e., the vitreous body, the lens or the cornea, in a surgical operation on them. The means comprises fine particles of a macromolecular compound, in particular, those one gram of which cannot be dissolved in less than 30 mL of water within 30 minutes at 20° C., and whose average particle size is 0.01-500 μm, and which, among others, is a biodegradable macromolecular compound and/or a water soluble macromolecular compound.
CN101113134A Triterpenes anti-neoplastic compound in cambric asterism sponge and method for preparing the same The invention relates to the medicine technical field, in particular to an antineoplastic triterpene compound of C30H42O4 obtained from a separation from Stelletta tenui, which comprises two structures, the transverse and cis structures, respectively named Stellettin L and Stellettin M and with the chemical structure formula of C30H42O4. According to analysis of various modern spectrums, in particular to comprehensive analysis of various advanced dimension nuclear magnetic resonance spectra, the chemical structure and solid form of the compound can be determined. The vitro antineoplastic test shows that the two compounds have evident controlling effect to four neoplastic cell lines such as A549 stomach cancer cell and SMMC-7721 liver cancer cell, etc.; the invention provides a pioneer compound for study of new antineoplastic medicine and has important value for development of marine medicine resources.
WO2011044506A2 Sulphone compounds and methods of making and using same The invention provides sulphone compounds according to formula (Ia) and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
US20100279997 Analgesic that binds filamin a A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.
CN101747226A N-oxalic acid acyl amino acid derivatives and N-oxalic acid acyl dipeptide derivatives as well as applications thereof in preparation of consciousness-promoted drugs The invention relates to N-oxalic acid acyl amino acid derivatives and N-oxalic acid acyl dipeptide derivatives as well as applications thereof in the preparation of consciousness-promoted drugs. The derivatives are shown in the formulas I-IV, have the functions of lowering brain waves delta and stigmatic indexes and increasing theta indexes, and can be applied to the preparation of the consciousness-promoted drugs.
US20110130402 Heteroaromatic glucokinase activators The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators which increase insulin secretion for the treatment of type II diabetes.
CN101450074B Composition capable of greatly improving gastrointestinal tract function and preventing and treating astriction The invention relates to a health-care food preparation, namely a composition for obviously improving gastrointestinal tract function and preventing and treating constipation, the preparation is prepared by xylo-oligosaccharide, biological calcium carbonate, vitamin C and milk essence based on regulated proportion. The composition of the invention has function for improving the gastrointestinal tract (loosening the bowel to relieve constipation) proved by the detection through health-care food function detection center, college of arts & science of Beijing union university.
WO2008078797A1 Sodium absorption inhibitor, potassium absorption inhibitor, phosphorus absorption inhibitor and preventive agent, therapeutic agent and food containing the same A sodium absorption inhibitor, a potassium absorption inhibitor, and a phosphorus absorption inhibitor, each of which contains as an active ingredient, a metal salt of a cross-linked cellulose derivative represented by the following general formula (I), and a preventive agent, a therapeutic agent and a food for diseases caused by overconsumption of table salt, potassium and phosphorus or diseases which require restriction of intake of table salt, potassium, and phosphorus are provided. With the use of them, overconsumed table salt, potassium, and phosphorus can be actively and safely excreted outside the body. R-O-A (I) (In the formula (I), R represents a cross-linked cellulose residue, and A represents a functional group a having a cation exchange ability.)
CN103301180A Selenium-enriched ganoderan and preparation method thereof The invention discloses selenium-enriched ganoderan and a preparation method thereof. The raw material of the polysaccharide liquid comprises the following components in parts by weight: selenium-enriched lucid ganoderma, cordyceps militaris, pollen pini, pigeonpea and ginseng, wherein the use level of selenium-enriched lucid ganoderma is greater than sum of those of cordyceps militaris, pollen pini, pigeonpea and ginseng. According to the invention, the principle of compatibility of the raw materials in a nutritional liquid is adequately considered by means of officinal characteristics of the materials, and the pointed components mutually complement, cooperate with each other and match and add with each other, so that the ganoderan disclosed by the invention has better anti-cancer effect, protects liver and detoxifies, enhances the cardiac function and prevents neurasthenia compared with those of independent lucid ganoderma, and the anti-cancer effect is remarkably enhanced. The ganoderan has the anti-aging effect, enhances the immunity and strengthens the absorption effect of vitamins. The ganoderan disclosed by the invention exerts the function of inhibiting generation of cancer cells by enhancing the immunity of human body, being directly effected to and killing cancer cells, and intercepting blood supply of tumor areas and differentiating cancer cells while eliminates the acceleration of ginseng to cancer cells.
US7696234 Histamine H3 receptor agents, preparation and therapeutic uses The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
WO2011005052A2 Novel arylpiperazine-containing imidazole 4-carboxamide derivatives and pharmaceutical composition comprising same A novel arylpiperazine-containing imidazole 4-carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a depressive disorder are provided.
US20130040992 Substituted 2, 6-Diamino-3, 5-Dicyano-4-Aryl-Pyridines And Their Use As Adenosine-Receptor-Selective Ligands The present invention relates to substituted 2,6-diamino-3,5-dicyano-4-arylpyridines of the formula (I) wherein the definitions of substituent groups R1-R7 are as provided in the specification and claims, to a pharmaceutical composition containing such a compound, to a process for preparation of such materials, and to their use as medicaments for the treatment of cardiovascular disorders and diabetes.
WO2009115321A8 Imidazopyrimidine, imidazopyrazine and imidazopyridazine derivatives as melanocortin-4 receptor modulators The present invention relates to substituted imidazopyrimidine derivatives, substituted imidazopyrazine derivatives and substituted imidazopyridazine derivatives as melanocortin-4 receptor (MC-4R) modulators, in particular as melanocortin 4 receptor antagonists. The antagonists are useful for the treatment of disorders and diseases such as cachexia induced by e.g. cancer, chronic kidney disease (CKD) or chronic heart failure (CHF), muscle wasting, anorexia induced by e.g. chemotherapy or radiotherapy, anorexia nervosa, amyotrophic lateral sclerosis (ALS), pain, neuropathic pain, anxiety and depression, nausea and emesis. Formula (I).
US8287894 Hyaluronan as a drug pre-sensitizer and chemo-sensitizer in the treatment of disease This application provides methods and compositions for the treatment of cancer. The application provides compositions comprising hyaluronic acid and a chemotherapeutic agent such as irinotecan that are useful in the treatment of cancer.
US20080226661 Using immunoaffinity recognition to identify phage clones expressing mycoplasma peptides; developing vaccines for prevention and treatment of contagious bovine pleuropneumonia The present invention relates to a method for identifying an agent for potential use in a vaccine. The present invention also provides agents identified by this method for use in a vaccine. The present further describes peptides of the pathogen Mycoplasma for use as a vaccine to treat or present diseases caused by Mycoplasma species, such as, Contagious bovine pleuropneumonia (CBPP).
CN103690506A Trospium chloride slow-release composition and preparation method thereof The present invention provides a trospium chloride slow-release composition and a preparation method thereof. According to the trospium chloride slow-release composition, an active drug component trospium chloride, an enteric material and a slow-release material are directly mixed according to a specific ratio so as to be adopted as a slow-release coating layer, such that rapid-release, slow-release and enteric delayed-release can be integrated, the drug release behavior and the blood drug level are stable, the toxic-side effect is reduced, and the treatment effect is good. The trospium chloride slow-release composition comprises, by weight, 40-60 parts of a blank pill core, 20-30 parts of a drug loading layer wrapped on the blank pill core, 1-5 parts of a separation layer wrapped on the drug loading layer, and 20-30 parts of a slow-release coating layer wrapped outside the separation layer, wherein the active drug of the drug loading layer is trospium chloride, and the slow-release coating layer comprises, by weight, 19-26 parts of a slow-release material, 0.8-1.8 parts of an enteric material and 0.2-1.2 parts of trospium chloride.
CN101926819A Compound polyhexamethylene guanidine complexing iodine disinfector and preparation method thereof The invention relates to a compound polyhexamethylene guanidine complexing iodine disinfector and a preparation method thereof. The compound polyhexamethylene guanidine complexing iodine disinfector comprises the following components in percentage by mass: 0.1-0.5 percent of polyhexamethylene guanidine, 0.5-5 percent of PVP-I (polyvinylpyrrolidone iodine), 30-70 percent of ethanol, 0.1-1 percent of non-ionic surface active agent, 0.5-3 percent of skin-protecting agent, 0.05-0.2 percent of citric acid and the balance of water. The preparation method of the compound polyhexamethylene guanidine complexing iodine disinfector comprises the following steps of: adding polyvinylpyrrolidone iodine into the water according to the content and the components, and stirring the mixture to dissolve; sequentially adding the non-ionic surface active agent, the skin-protecting agent and the citric acid, and stirring the mixture to dissolve; adding and stirring ethanol to the mixture uniformly; and adding and stirring polyhexamethylene guanidine to the mixture uniformly to obtain the compound polyhexamethylene guanidine complexing iodine disinfector. The compound polyhexamethylene guanidine complexing iodine disinfector has the characteristics of stable characteristics, quick and lasting sterilization function, low simulation to skins, quick drying and convenient use.
WO2012105467A1 Oligonucleic acid composition and antiallergic agent An oligonucleic acid composition which contains: an oligonucleic acid having antiallergic activity and antimicrobial activity (such as an siRNA that suppresses transcription factor NF-κB); a cell-penetrating peptide (a basic peptide which comprises arginine, histidine, and cysteine at both ends and which is modified with a higher fatty acid); and if necessary, a tight junction opening peptide. The cell-penetrating peptide may electrostatically form a composite with the oligonucleic acid, or may form a crosslinked composite by a disulfide bond. Since the oligonucleic acid composition has high stability of the oligonucleic acid, high cutaneous permeability and high mucosal permeability and is thus capable of delivering an oligonucleic acid to a target cell, allergic diseases and infectious diseases can be effectively treated by administration of the oligonucleic acid composition through skin or mucosa.
CN102302485A Purposes of flavane derivatives The invention relates to purposes of flavane derivatives, and specifically relates to the purposes of flavane derivatives represented by a formula VI in the preparations of anti-anoxia medicines and anti-anoxia health products. The invention also relates to the purposes of the compounds in preparing the medicines used for preventing and/or treating various hypoxic diseases, or in ameliorating andrelieving various malaise symptoms related to anoxia under hypoxia environments. The formula VI is shown below.
CN102805740A Rivastigmine capsules and preparation method thereof The present invention relates to rivastigmine capsules and a preparation method thereof. The capsule contains rivastigmine adopted as an active ingredient, hydroxy propyl methyl cellulose adopted as a binder and a film forming material, and other medicinal auxiliary materials. The preparation method comprises: adopting a fluidized bed process to prepare particles, and further adopting hydroxy propyl methyl cellulose to carry out coating on the particles, wherein the prepared product has characteristics of low hygroscopicity and good storage stability so as to easily store the product, and the particles prepared according to the method of the present invention have characteristics of good fluidity and uniform particle size distribution. In addition, the preparation process is stable, quality is controllable, and various detection indexes of the finished product meet requirements, such that low production cost is ensured, and the method is suitable for industrial production.
WO2013146376A1 Coating composition and medical device The present invention provides a coating composition for drug eluting medical devices, which is capable of forming a medical agent coating layer that is not easily separated on the way to a target tissue during the delivery. This coating composition contains: a water-insoluble medical agent; at least one substance that is selected from the group consisting of hyaluronic acid, alkanoylated hyaluronic acid obtained by substituting at least some of hydrogen atoms in the hydroxy groups of hyaluronic acid with alkanoyl groups, and salts of hyaluronic acid and the alkanoylated hyaluronic acid; and at least one substance that is selected from the group consisting of amino acid esters and salts thereof.
WO2011038207A1 Phosphorus-containing thyroid hormone receptor agonists and methods of use The present invention relates to sulfonic acid containing compounds that bind to thyroid receptors in the liver. Activation of these receptors results in modulation of gene expression of genes regulated by thyroid hormones. The compounds can be used to treat diseases and disorders including metabolic diseases such as NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, and metabolic syndrome X.
CA2233677C A novel combination of a .beta.-receptor blocker and an opioid New combination of a .beta.-receptor blocker or a pharmaceutically acceptable salt thereof, and an opioid or a pharmaceutically acceptable salt thereof, optionnally in the presence of a pharmaceutically acceptable carrier or any additional agents which may be active or inactive.The new combination confers a synergistic effect, and provides unexpected efficacy in the treatment of pain.
EP1605927B1 Anti-microbially active diamine-based guanine derivatives The invention relates to the use of a polymer guanine derivative based on a diamine comprising oxyalkylene chains between two amino groups, whereby the guanine derivative is a product of polycondensation of a guanidine acid addition salt with a diamine comprising polyakylene chains between two amino groups, used in the production of an antimicrobially active medicament.
US20140073603 Phenylboronic Acid The present invention relates to a specific phenylboronic acid compound having anti-cancer, anti-inflammatory, and anti-microbial activity, in addition to a pharmaceutical composition comprising the same. The present invention also discloses a process for preparing said compound. The compound is represented by the formula (I):
CN102015701A PIM kinase inhibitors and methods of their use The present invention relates to new compounds of Formulas (I) and (II), their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pirn kinase activity and/or the prophylaxis or treatment of cancer.
CN103070827A Method for preparing tulathromycin soluble powder The invention relates to tulathromycin soluble powder used for treating chicken Escherichia coli disease. A preparation method comprises the steps that: a tulathromycin salt compound is well mixed with a carrier; the mixture is crushed and sieved by using a 80-mesh sieve, such that a product is obtained.
US20100047368 Compositions and methods for the treatment or prevention of chemoresistant neoplasia The invention generally features compositions and methods useful for the treatment and diagnosis of a neoplasia in a subject. In particular, the invention provides therapeutic compositions that decrease the expression of an Nfr2 nucleic acid molecule or polypeptide for the treatment of a neoplasia, such as a chemoresistant neoplasia, in a subject.
WO2011081612A1 Use of krypton or xenon as an antiviral agent The present invention relates to the field of agents for combating viruses and can be used in medicine, pharmacology, the foods industry and in other sectors where there is the need for neutralizing viruses. The use of krypton or xenon as an antiviral agent ensures a broad field of use of said agent as, for example: a disinfectant, an antiseptic, and a drug, wherein the use does not result in irreversible changes (physical or chemical) in the object being treated because of the chemical inertness of the agent, and makes it possible to use said agent both for treating goods, including food products, and for humans and animals both enterally and parenterally. Taking into consideration the fact that krypton and xenon are gases, this makes it possible to use said gases not only in forms which are traditional for these purposes, namely liquid forms (such as a disinfectant or antiseptic or a drug) and solid forms (a drug), but also in the form of aerosols, which provides for the treatment of both external and internal cavities simultaneously and, importantly, in humans as well as animals.
WO2008125891A3 Pyrimidinyl-piperazines useful as dopamine d3 /d2 receptor ligands The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein Rl, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.
US20100137347 5-[3-((1S,2R)-2-{4-[1-(4-Methoxy-benzyloxy)-hexyl]-phenyl}-3-methylene-cyclopentyl)-propyl]-thiophene-2-carboxylic acid methyl ester; glaucoma, inflammatory bowel disease, the stimulation of hair growth, and the stimulation of the conversion of vellus hair to terminal hair Disclosed herein is a compound of the formula (I). Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.
WO2013071009A1 4 - pregenen- 11ss - 17 - 21 -triol-3, 20 -dione derivatives for the treatment of ocular conditions The present invention relates to novel 4-pregenen-11-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation.
WO2005000308A3 Methods of identifying hcv ns5b polymerase inhibitors and use against hepatitis c The present invention relates to a variety of screening methods, utilizing both biochemical and cellular assays as well as in silico assays, for use in the discovery of agents active in the treating or preventing Hepatitis C virus (HCV) infections. The invention also relates to methods of inhibiting an HCV NS5B polymerase and to the treatment and/or prevention of HCV infections with compounds having specified binding properties.
CN102600211A Complex fermentative cordycepic fungal powder curcumin combined medicine The invention relates to complex fermentative cordycepic fungal powder curcumin combined medicine, and discloses a weight ratio of all raw material compositions of the complex fermentative cordycepic fungal powder curcumin combined medicine. The invention provides a preparation method of the complex fermentative cordycepic fungal powder curcumin combined medicine. The complex fermentative cordycepic fungal powder curcumin combined medicine is made into capsules, granules and tablets according to an allowed dose of pharmacy. The complex fermentative cordycepic fungal powder curcumin combined medicine is used for resisting aging, fatigue, shock and light radiation, for sedation, for resisting oxygen deficiency and for improving the immunity.
US20080234245 Angiostatic Agents for Controlling Choroidal Neovascularisation After Ocular Surgery or Trauma Compositions of angiostatic agents for treating choroidal neovascularization resulting from ocular surgery or from trauma to ocular tissue and methods for their use are disclosed.
US20120316148 Compositions and Methods for Modulating a Kinase The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.
CN1883499A Drip pills of mangiferin and preparation method thereof The invention relates to mangiferin dropping pills and process for preparation, wherein the dropping pills are prepared from high purity mangiferin as the pharmacological active constituent and auxiliary material as the matrix. The dropping pills have hepatoprotective action.
CN101786992B 2-hydroxymethyl-3,5,6-trimethylpyrazine derivatives, preparation methods and application thereof The invention provides 2-hydroxymethyl-3,5,6-trimethylpyrazine derivatives with the structure of a formula (I) or pharmaceutically acceptable salts thereof, relating to the field of related antithrombotic medicines, wherein the definition of R is shown in the specification of the invention. The invention also provides preparation methods of the derivatives or pharmaceutically acceptable salts thereof, medicine compositions and application of the derivatives used as effective components in preparing medicines for treating cerebral thrombosis, cerebral infarction, angina, myocardial infarction and arrhythmia related with thrombus.
CN103191060A Amphipathic carboxymethyl glucan-modified magnetic lipidosome, and preparation and application methods thereof The invention belongs to the field of a nanotechnology and in particular relates to an amphipathic carboxymethyl glucan-modified magnetic lipidosome, and preparation and application methods thereof. The magnetic lipidosome is prepared by a film ultrasonic dispersion method and the surface of the magnetic lipidosome is modified by amphipathic carboxymethyl glucan, so high stability is achieved. The amphipathic carboxymethyl glucan can be synthesized by oleylamine and glucan. The magnetic lipidosome has small grain size, dispersion uniformity, high stability and high magnetic responsiveness. The magnetic lipidosome can serve as a thermal therapy medium and a nuclear magnetic resonance imaging contrast agent and also can be used for carrying medicines in a targeted mode and controllably releasing medicines. The magnetic lipidosome has simple and practical preparation process, low cost and excellent biocompatibility and biodegradability, accords with the requirements of green chemistry, and has a wide clinical application prospect.
US20080070901 Cholineterase inhibitors for treating inflammation A method of treating a subject with a cytokine-mediated inflammatory disorder comprising administering to the subject an effective amount of a pharmaceutically acceptable cholinesterase inhibitor, provided that the inhibitor is not galantamine.
CN103724374A Benfotiamine compound, preparation method and pharmaceutical composition containing benfotiamine compound The invention relates to a benfotiamine compound, a preparation method and a pharmaceutical composition containing the benfotiamine compound, and belongs to the technical field of medicines. The compound has a chemical structural formula shown as (img file='DDA0000454523390000011.TIF' wi='1320' he='570' /); and a X-ray diffraction pattern of the benfotiamine compound is as shown in figure 1. The preparation method comprises the following steps of: adding crude benfotiamine and purified water to a reaction flask; dropping proper amount of alkaline solution; heating to 60 to 90 DEG C, wherein the temperature of 70 to 80 DEG C is better; dropping dilute acid to regulate pH (Power of Hydrogen) to be 3.5 to 4.0; adding a mixed solvent of ethanol, dimethylformamide and chloroform; controlling the temperature to be 60 to 90 DEG C, wherein the temperature of 70 to 80 DEG C is better; growing the grain; performing suction filtration; cleaning the gain with purified water and acetone in sequence; performing vacuum drying to obtain the finished product of benfotiamine. The benfotiamine is a novel crystal compound which shows an obviously improved solubility; in addition, a benfotiamine tablet prepared from the benfotiamine compound is high in dissolubility.
US20100290982 Solid in oil/water emulsion-diffusion-evaporation formulation for preparing curcumin-loaded plga nanoparticles The present invention includes compositions and methods of making an activated polymeric nanoparticle for targeted drug delivery that includes a biocompatible polymer and an amphiphilic stabilizing agent non-covalently associated with a spacer compound that includes at least one electrophile that selectively reacts with any nucleophilic on a targeting agent and places the targeting agent on the exterior surface of a biodegradable nanoparticle, wherein an active agent is encapsulated in or about the nanoparticle.
CN102151252A Glipizide osmotic pump type controlled release tablet The invention provides a glipizide osmotic pump type controlled release tablet. The controlled release tablet adopts ethylene cellulose and polyvidone as semi-permeable membrane materials and is unsymmetrical in appearance, not only can overcome the defect that a semi-permeable membrane is aged and reduce the drug release residue, but also can simplify the identification of laser drilling and is stable to place when being conveyed on a conveyor belt; and a hole is easier to be drilled in the middle to facilitate the stable release of the drugs. The invention also provides a method for improving the aging resistance of the glipizide osmotic pump type controlled release tablet, which is characterized in that the ethylene cellulose-the polyvidone is adopted as the semi-permeable membrane material. In addition, the invention further provides an application of an ethylene cellulose-the polyvidone combination for preparing the aging resistance of the glipizide osmotic pump type controlled release tablet.
CN103735512A Enrofloxacin solid dispersion and preparation method thereof The present invention relates to an enrofloxacin solid dispersion, wherein enrofloxacin is adopted as a main component and is uniformly mixed with a water soluble carrier, the obtained mixture is heated so as to be converted into a completely-transparent liquid, and then low-temperature curing, vacuum drying and crushing are performed to prepare the finished product. According to the present invention, the finished product is the solid powder, such that the finished product can be directly and orally taken by animals during use or can be directly prepared into an injection or an oral liquid so as to be used, and does not have adverse reactions, and the single-dose concentration is high so as to provide characteristics of rapid disease treatment and treatment period shortening.
US20090092641 Uses of natural immunobiotic extract The present invention provides a method of improving disease management in an animal by administering an effective amount of β-glucan composition to the animal. The β-glucan composition comprises at least about 70% β-(1,3/1,6)-D-glucan by dry weight and a biological activity of at least 20 μg Bb released per mg of β-(1,3/1,6)-D-glucan. The method may also result in beneficial secondary effects including an increase in growth efficiency of the animal; an increase in the survival rate of the animal; an increase in the colostrum quality of the animal; and any combination thereof. The β-glucan composition may also be administered in combination with or prior to a vaccine, leading to an increase in antibody formation; the negative growth responses associated with administration of a vaccine may also be reduced. In the present method, the β-glucan composition may be administered in combination with an animal feed.
CN101049308A Solid dispersion containing rimonabant and polyethyleneglycol, preparation and medication application A dispersed solid composition used to prepare medicines with high wettability and water-solubility is prepared from Limonaban and ethanediol. Its preparing process is also disclosed.
US20080050387 Non-Androgen Dependent Roles for Androgen Receptor and Non-Androgen Related Inhibitors of Androgen Receptor Disclosed are compositions and methods for modulating AR activity, such as non-androgen dependent AR activity. Also disclosed are compositions and methods for diagnosing beast cancer and for inhibiting breast cancer growth. In addition, disclosed are methods for identifying molecules that inhibit AR in non-androgen dependent ways.
US20120270848 Novel Compositions and Therapeutic Methods Using Same The present invention includes compositions and methods for treating a subject in need of opioid therapy, wherein the opioid therapy produces or has the possibility of producing respiratory depression or a breathing control disorder in the subject.
CN101007138A Drug for treating male infertility The invention discloses a medicament for treating male infertility, which is prepared from astragalus root, Siberian solomonseal rhizome, epimeddium, cnidium fruit, plantain seeds, ginseng, raspberry, deer horn gum, asparagus root, poria cocos, leek seeds, broomrape, anemarrhena rhizome and eucommia bark through steps of disintegrating, grilling, extracting concrete, and the medicament can be prepared into powders, granules, tablets or capsules.
US20090264427 3-Cyanoquinolines, Methods for Preparation and Use as Insulin-like Growth Factor Inhibitors Imidazole-substituted 4-anilino-3-cyanoquinolines are described, which selectively inhibit IFGR kinase activity and are useful for treating disorders associated with IGFR kinases.
CN101164557B Medical composition for preventing and/or treating bone matrix's loss The present invention relates to a medicine composite for effectively curing osteoloss. Said medicine composite is formed from licorice, black soybean, cnidium seed and deerhorn with effective dose.
EP2425715A1 Treating symptoms of renal disease with selective androgen receptor modulators (SARM) This invention provides: 1) a method of treating a subject suffering from, or predisposed to a kidney disease or disorder; 2) a method of treating a subject suffering from a wound, or reducing the incidence of, or mitigating the severity of a wound in a subject; 3) a method of treating a subject suffering from a burn, or reducing the incidence of, or mitigating the severity of a burn in a subject, comprising the step of administering to said subject a selective androgen receptor modulator (SARM) compound; 4) a method of treating a subject suffering from a spinal cord injury, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.
CN1827162A Animal medicine capable of resisting multiple irritated stress of chicken The invention relates to a animal medicine for resisting various chicken irritability characterized by that, each 1000ml contains 500-5000mg solution of alpha-mannosan peptide, the solution is prepared through subjecting preferred alpha-hemolytic streptococcus 33# to space embarkation, using fine bacteria through space mutagenesis seed selection as the production bacterial, carrying out first level fermentation and second level fermentation to produce mannosan peptide fermentation liquor, purifying and filtering the fermentation liquor, charging right amount of perfume compound and flavoring agent, dissolving, stirring homogeneously and filtering again, loading and sealing, heat pressing and sterilizing. Each 1000ml of the obtained solution contains alpha-mannosan peptide 500mg, vitamin C 10-200g.
CN101129541A Medicament for treating bone joint disease The invention discloses a medicament for treating waist and leg pains, wherein the oral administration dose form is prepared from the following raw materials (by weight portion): wild or spiny jujuba root 12-18 parts, fig root 12-18 parts, nodular branch of pine 12-20 parts, and the externally used dose form is prepared from the following raw materials (by weight ratio): purslane 370-430 parts, pumpkin vine 270-330 parts, fresh ginger 220-280 parts, Chinese mugwort leaf 270-330 parts, safflower 130-170 parts, ledebouriella root 370-430 parts. The externally used medicament can also comprise seabuckthorn fruit 450-550 parts, Indian mallow 270-330 parts, mulberry twig 450-550 parts, willow branch 450-550 parts, pine 450-550 part.
CN1958617A Tea polysaccharide, preparation method, and usage This invention relates to tea polysaccharide, which is prepared by: (1) pulverizing tealeaves or cutting into 1-2 cm segments; (2) extracting with water for 1-4 times, incorporating the extract, filtering, precipitating the filtrate with 1-3 volume times of 45-99% ethanol, centrifuging to separate the precipitate, and dissolving the precipitate with water to obtain aqueous solution; (3) passing through 0.1-0.3 mum ultra-filtration membrane; (4) intercepting the ultra-filtration solution to obtain interception solution with the intercept molecular weight of 2000-100000; (5) adsorbing and separating the interception solution with an adsorption column filled with adsorption material, and freeze-drying to obtain tea polysaccharide. The purity of tea polysaccharide is high, and the preparation method is simple, thus is suitable for mass production. The tea polysaccharide can be used for manufacturing drugs for treating diabetes, hyperlipemia and hyperglycemia.
CN1660115A One step method for synthesizing asepsis powder of Cefathiamidine A process for preparing the aseptic powder of cefathiamidine includes such steps as dissolving 7-bromoacetyl ACA, triethylamine and N,N-diisopropyl thiourea in dichloromethane, ultrafiltration, aseptic stirring while reacting, dropping acetone, crystallizing, filtering and baking.
WO2009035068A1 Novel 1,3,3-trimethyl-7-phenyl-3,4-dihydro-1h-quinoxalin- 2-one derivatives The invention provides novel 1,3,3-trimethyl-7-phenyl-3,4 -dihydro-1H-quinoxalin-2-one derivatives represented by the general formula (1), salts thereof, and pharmacological effects of the same. The derivatives and salts thereof are useful as glucocorticoid receptor modulators, particularly, remedies for diseases against which glucocorticoid receptor agonists such as steroids are efficacious, for example, inflammatory bone and joint diseases and inflammatory eye diseases (anterior or posterior eye inflammatory diseases): [Chemical formula 1] (1) (2a) (4a) (3a) (5a) wherein R1 is a group represented by the general formula (2a), (3a), (4a) or (5a); R2 is lower alkyl or the like; R3 is hydrogen, lower alkyl, cycloalkyl, aryl, a heterocyclic group, aralkyl, or the like; R4 and R5 are each hydrogen, lower alkyl, or the like; A is lower alkylene; R6, R7, R8 and R9 are each halogeno, lower alkyl, hydroxy, lower alkoxy, or the like; and m, n, p and q are each 0, 1 or 2.
CN1771996A Effervescent pearl tablet and its prepn The present invention provides one kind of effervescent pearl tablet, and the effervescent pearl tablet consists of pearl powder, vitamin C and edible supplementary material. The effervescent pearl tablet can replenish human body with nutritious component Ca and vitamin C, and is safe in application.
CN101578091A Composition for external application to skin Disclosed is a composition for external application to skin which is characterized by containing one or more compounds selected from the group consisting of an aminoacetamide compound represented by the general formula (1) below and salts thereof.
WO2011107585A1 Morpholino substituted urea derivatives as mtor inhibitors The invention relates to compounds of formula (I) wherein X1, X2, R1 to R4, m, n have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
US20110015120 Pharmaceutical and cosmetic compositions including lactoferrin, ciclopirox, etidronic acid Pharmaceutical and cosmetic compositions for topical use comprising Lactoferrin, Ciclopirox and/or salts thereof, Etidronic Acid and/or salts thereof and use of said compositions in the treatment of dermatological disorders and conditions such as seborrheic dermatitis and dandruff.
CN101433543A Compound mequindox injection The invention discloses compound mequindox injection, and belongs to medicine preparation containing organic components, or anti-infective medicament for livestock. The injection of each 1, 000 liters is prepared by the following raw materials: 100 to 400 kilograms of sodium salicylate, 10 to 150 kilograms of mequindox, 5 to 110 kilograms of gentamicin sulphate, 1 to 20 kilograms of atropine sulfate, 1 to 20 kilograms of chlorphenamine maleate, and the balance being water for injection. The injection adopts combined compound preparation of the mequindox and the gentamicin sulphate, has efficiency and high efficiency for pig bacterial diarrhea, treats both symptoms and root causes, and relieves stress reaction of sick livestock body.
US20080182855 Antibacterial Quinoline Derivatives The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of a bacterial disease including a mycobacterial disease, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of bacterial diseases and a process for preparing the claimed compounds.
EP2164492B1 Trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine for treating schizophrenia The present invention relates to use of (thio)-carbamoyl-cyclohexane derivatives, particularly trans-4- {2-[4-(2,3 -dichlorophenyl)-piperazin-1-yl] -ethyl} -N,N- dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment of schizophrenia. Furthermore, the present invention relates to the treatment of schizophrenia through the administration of (thio)- carbamoyl cyclohexane derivatives, particularly trans-4- {2-[4-(2,3-dichlorophenyl)-piperazin- 1-yl] -ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof.
CN103330840A External unguent for treating burn and preparation method thereof The invention discloses an external unguent for treating burn. The unguent comprises the following raw materials in parts by weight: 20-30 parts of sensitive plant, 10-15 parts of lithospermum, 10-15 parts of golden cypress, 10-12 parts of peperomia dindygulensis miq, 6-10 parts of flos paulowniae, 10-14 parts of ophiopogon root, 10-13 parts of radix rehmanniae recen, 8-10 parts of dandelion, 10-14 parts of fried garden burnet, 10-13 parts of pseudo-ginseng, 6-8 parts of flowers carthami, 3-4 parts of the root of kudzu vine, 3-5 parts of madder, 4-7 parts of Coptis chinensis, 10-12 parts of rhizoma bletillae, 8-11 parts of rhizoma atractylodis, 10-13 parts of Ixeris japonica, 6-7 parts of mint, 2-3 parts of Elaeagnus, 3-4 parts of liquorice, 8-10 parts of ash bark, 4-5 parts of dried alum, 10-15 parts of rosin, 6-10 parts of radix sophorae flavescentis, 6-10 parts of smoked plum, 10-12 parts of borneol, 200-260 parts of sesame oil and 100-150 parts of beewax. The unguent disclosed by the invention has the effects of preventing bacteria, diminishing inflammation, relieving pain, eliminating swelling and resisting irritability. The infection probability is low, and the burn is not specially treated. The unguent has low sterile demand to the trauma and is simple in using method. The unguent is not combined with other antibiotics, and the unguent is short in curative period, quick-acting and free from scars.
US20120004249 The polymorph forms of 4-anilinoquinazoline derivatives, the preparation methods and uses thereof The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof.
WO2014024164A1 Process for the preparation of pemetrexed and lysin salt thereof The present invention refers to a process for the synthesis of pemetrexed and salts thereof, in particular to a lysine salt thereof, to said salt as such and to pharmaceutical compositions that comprise the same. Furthermore, the present disclosure also relates to a crystalline form of the synthesis intermediate pemetrexed diethyl ether and a crystalline form of the pemetrexed lysine salt.
US20070244102 Combination of Dermaciclane and Opoids as Analgesics The invention relates to a combined analgesic pharmaceutical composition which comprises as component: A) (1R,2S,4R)-(−)-2-[N,N-(dimethylaminoethoxy)]-2-phenyl-1,7-7-trimethylbicyclo[2.2.1]heptane or a pharmaceutically acceptable acid addition salt thereof and as component B) morphine, an opioide type analgesic and/or a non-opioide type analgesic in admixture with suitable pharmaceutical carriers and/or auxiliary agents. Deramciclane increases the analgesic effect of morphine.
CN102648914A Use of caffeine in preparation of medicine for treating Senile Dementia The invention relates to a use of caffeine in preparation of medicine for treating Senile Dementia. The use of caffeine in preparation of medicine for treating Senile Dementia, disclosed by the invention, has the advantage that a better treatment method and medicine are provided for treating Senile Dementia; and compared with the former medicine for treating Senile Dementia, caffeine has the characteristics of less side effects and remarkable curative effect.
WO2009092442A1 Treatment of portal hypertension and related conditions by combined inhibition of the vegf and pdgf signalling pathways The present invention relates to the treatment and/or prevention of portal hypertension and manifestations related thereof, by the inhibition of both platelet-derived growth factorand vascular endothelial growth factor signalling pathways. Combinations of VEGF and PDGF signalling pathways inhibitors are disclosed for the treatment and/or prevention of portal hypertension, e.g. rapamycin and imatinib, sorafenib.
US20090233893 Methods of Dissolving Beta-Sheet Proteins and Uses Thereof The application discloses metallized chelator complexes and uses of metallized chelator complexes for dissolving β-sheet proteins and reducing formation of β-sheet proteins, where the metallized chelator complex comprises a metal ion chelator and a metal ion.
CN102935229A New medical application of metallic simple substances The invention provides new medical application of metallic simple substances. More specifically, the invention provides application of metallic simple substances in preparation of drugs for treating and/or preventing vitamin B12 associated diseases or symptoms and in methods for treating and/or preventing vitamin B12 associated diseases or symptoms. The diseases or symptoms include tumors, which can be benign and malignant tumors. The metallic simple substances include metallic cobalt, metallic copper and the like.
CN101474344B Qi-moving dampness-drying spleen-strengthening medicament for sheep The invention relates to a medicine for sheep, in particular to a medicine which comprises botanical drugs and inorganic salt, is eaten by the sheep and can promote circulation of Qi, eliminate dampness and invigorate the spleen. The composition of the medicine is: 4 parts of dried orange peel (parts by weight, the following are the same), 4 parts of rhizoma atractylodis, 4 parts of pipewort, 3 parts of white vitriol, 3 parts of Chinese arborvitae twig, 3 parts of bark of elm tree, 2 parts of garlic, 2 parts of Kuan Chung ( Herb of Shiny Cinquefoil), 1 part of folium cortex eucommiae and 1 part of fennel. The medicine of the invention has the advantages of promoting circulation of Qi and reinforcing the stomache, helping digestion and increasing weight of the sheep and strengthening fodder and improving meat quality of the sheep.
WO2007126043A1 Use as drugs of carboxylic acid derivatives having thiazole rings [PROBLEMS] To provide compounds useful as preventive and/or therapeutic drugs for diabetic hyperlipemia. [MEANS FOR SOLVING PROBLEMS] The invention has been accomplished on the basis of a finding that compounds represented by the general formula (I) have plasma TG decreasing effect, free fatty acid decreasing effect and serum HDL cholesterol increasing effect on various parameters of diabetic hyperlipemia: (I)
CN103223061A External application bedsore drug and preparation method thereof The present invention discloses an external application bedsore drug, which is prepared from the following raw materials: 20-35 g of drynaria, 15-30 g of euphorbia humifusa, 100-120 g of longleaf garden burnet root, 50-70 g of amur corktree bark, 90-115 g of propolis, 20-35 g of kalopanax septemlobus root, 15-25 g of coptis chinensis, 15-20 g of licorice root, 9-13 g of largeleaf gentian root, 3-5 g of kusnezoff monkshood mother root (processed), 15-30 g of linear stonecrop herb, 10-25 g of upright ladybell root, 30-50 g of baikal skullcap root, 30-60 g of nakedflower beautyberry branchlet and leaf, 15-25 g of syzygium buxifolium hook, 15-20 g of humus flava usta, 30-50 g of kweiyang betony herb or root, 10-25 g of vaiante spleenwort herb, 15-30 g of tree peony root bark, 3-6 g of borneol, 25-45 g of harlequin glorybower root, 10-20 g of bigfruit phymatopsis herb, 9-15 g of purpleflower holly fruit, 10-15 g of eucalyptus globules, 15-30 g of cairo morningglory root or leaf, 15-25 g of cudweed herb, 25-50 g of ass-hide gelatin, and 3000 ml of 50-65% alcohol.
CN103159636A Aminomethyl caproic acid derivative and use The invention discloses an aminomethyl caproic acid derivative and use, in particular a composition which comprises a compound shown by formula I and a compound shown by formula II as an impurity. The invention further discloses a medical preparation prepared by the composition and pharmaceutical use thereof. The compound provided by the invention has good pharmaceutical properties.
US20120231084 Galenic form suitable for absorbing, in a specific manner, the undesirable molecules in the digestive tract The present invention relates to a galenic form comprising particles capable of specifically adsorbing the undesirable molecules present in the digestive tract, to the method for preparing same and to the use thereof in particular for producing a medicine intended for preventing or treating undesirable effects linked to an imbalance of the intestinal and/or colonic flora that can result for example from treatment with antibiotics.
US8455510 Rapamycin carbonic ester analogues, pharmaceutical compositions, preparations and uses thereof Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.
DE4447972B4 Pharmaceutical preparations contg macrolide antibiotics - contain, as the carrier, a mixt of a hydrophilic phase, a lipophilic phase and a surfactant A pharmaceutical preparation comprises a macrolide and a carrier consisting of a hydrophilic phase, a lipophilic phase and a surfactant. Also claimed is a microemulsion preconcentrate carrier (or an agent suitable for oral use which is other than a cyclosporin) consisting of (i) a reaction prod. of castor oil and ethylene oxide; (ii) a re-esterification prod. of a plant oil and glycerine consisting mainly of mono-, di- and tri-glycerine of linoleic and oleic acid or a polyoxyalkylated plant oil; (iii) 1,2-propylene glycol; and (iv) ethanol. The pharmaceutical composition is in the form of an emulsion- or microemulsion-preconcentrate. The lipophilic phase comprises 10-85 wt.% of the carrier, the surfactant 5-80 wt.% of the carrier and the hydrophilic phase 10-50 wt.% of the carrier. The compositions pref. contain rapamycin class cpds. esp. FK506 in an amt. of 2-15 wt.%.
CA2066304C Pharmaceutical composition for the treatment of autoimmune diseases A pharmaceutical composition for the treatment of autoimmune diseases comprising an effective amount of a compound of formula A-CH2-O-CRR'-COOR''' (I) where A is the nucleus of 1-benzyl-indazol-3-yl, R and R', the same or different from each other, are H or an alkyl having from 1 to 5 carbon atoms, R''' is H or an alkyl having from 1 to 4 carbon atoms, or, when R''' is H, of a salt thereof with organic or inorganic pharmaceutically acceptable bases.
WO2010081341A1 The crystal form i of n-n-propyl-3-(4-methylphenyl) -4-(methylsulfonylphenyl)-2,5-dihydropyrrole-2-one and the preparation method thereof The crystal form I of N-n-propyl-3-(4-methylphenyl)-4-(4-methylsulfonylphenyl) -2,5-dihydropyrrole-2-one and the preparation method thereof. The method includes that any crystal forms or amorphous form of N-n-propyl-3-(4-methylphenyl)-4- (4-methylsulfonylphenyl)-2,5-dihydropyrrole-2-one are crystallized with polar organic solvents or their aqueous solutions to obtain the crystal form I of N-n-propyl-3-(4-methylphenyl)-4-(4-methylsulfonylphenyl)-2,5-dihydropyrrole-2-one. The obtained crystal form I of N-n-propyl-3-(4-methylphenyl)-4- (4-methylsulfonylphenyl)-2,5-dihydropyrrole-2-one has good crystal stability and chemical stability. The solvents used for crystallization has low toxicity and residue, so this crystal form I can used in the clinic with better effect.
US20080293652 Combination of Ad-P53 and Chemotherapy for the Treatment of Tumours The present invention relates to the use of p53 gene therapy to treat recurrent cancers in combination with a radio- or chemotherapy. Patients with recurring cancers are treated with a p53 expression construct followed by subsequent radio- or chemotherapy treatment. Viral and non-viral delivery systems, as well as various radio- and chemotherapy regimens are disclosed.
EP2012801A2 Gemcitabine combination therapy The present invention provides compositions and methods for the treatment of cell proliferative disorders using at least one DAC inhibitor and gemcitabine.
CN1602869A Dripping pills of eprazinone hydrochloride and its preparation The invention eprazinone hydrochloride pill, prepared by superfine crushing and pill producing techniques, can achieve the purposes of increasing disintegration and dispersion speeds, and dissolving-out speed and degree, quickly taking effect, improving drug stability, reducing auxiliary use, reducing production cost, being convenient to carry and take. Its compliance is good and it is especially suitable for children, the aged, patients in bed and patients difficult in swallowing to take.
CN1875940A Anticancer sustained release agent containing clorfarabine and its synergist Disclosed is a slow release agent containing clofarabine and synergistic agent, which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents include clofarabine and combination with clofarabine synergistic agent selected topology enzyme inhibitor and/or tetrazine compounds, the slow release auxiliary materials are selected from Polifeprosan, sebacylic acid copolymer, EVAc, polylactic acid and copolymer, polyethylene glycol mono methyl and copolymer, polyethylene glycol and polylactic acid copolymer, PLA-COOH or PLA-COOH/glycollic acid copolymer or their combination. The viscosity of the suspension adjuvant is 100-3000cp and is selected from sodium carboxymethylcellulose.
CN103239391A Tacrolimus ointment The invention provides a tacrolimus ointment composition and a preparation method of the tacrolimus ointment composition. The tacrolimus ointment composition provided by the invention has enhanced permeability and reduction of skin irritation, and can be used for the treatment of atopic dermatitis.
CN101797279A Health care product with dealcoholic function The invention discloses a health care product with dealcoholic function. The health care product contains L-arabinose and the root of kudzu vine. The health care product of the invention can be edible before drinking or when in drinking, has good taste and has good dealcoholic effect.
WO2008031842A1 Inhibitors of gpr87 for cancer therapy Use of GPR87 for the generation of GPR87 inhibitors. GPR87 inhibitors, e.g. anti-GPR87 antibodies and small molecules, are useful as drugs in the treatment of cancer. Methods for identifying small molecule GPR87 inhibitors employ cells transfected with GPR87 or GPR87-G-alpha fusion proteins.
EP0740701B1 Mammalian monocyte chemoattractant protein receptors DNAs encoding human chemokine receptors, MCP-1R and MCP-1RB, and processes for expressing them are disclosed. The receptor proteins, which are the products of alternately spliced versions of the MCP-1R gene, may be used in an assay to identify antagonists of MCP-1. The antagonists are therapeutically useful in the treatment of atherosclerosis and other diseases characterized by monocytic infiltrates.
WO2012163942A1 Substituted aminoimidazopyridazines The present invention relates to substituted aminoimidazopyridazine compounds of general formula (I) : in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
US20090253664 Combination andolast/glucocorticoids The invention relates to the combination of Andolast, a calcium-activated potassium channel opener and glucocorticoids for the treatment of patients suffering for airway diseases. Pharmaceutical compositions comprising Andoalst and glucocorticoids are also disclosed.
CA2126354C Use of 5-ht4 modulators for the manufacture of a medicament for the treatment of the bladder diseases A compound which acts as an antagonist at 5-HT4 receptors is of potential use in the treatment of conditions associated with bladder hypersensitivity, such as urinary incontinence, which is often associated with irritable bowel syndrome (IBS) and a compound which acts as an agonist at 5-HT4 receptors is of potential use in the treatment of conditions associated with a poorly functioning bladder, such as urinary bladder hypoactivity following prostectomy.
CN101322709B Medicament composition containing aripiprazole and preparation thereof The invention discloses a pharmaceutical composition containing aripiprazole and a preparation method thereof. The formula which is suitable for preparing oral disintegrating tablets provided by the invention comprises an active component, a disintegrating agent, a diluent agent and a latent solvent, a proper amount of a corrective, a lubricant and a glidant. The composition has simple formula, mature preparation process, and successfully solves the problem that oral disintegrating tablets can not be packed by using the common equipment in a way of choosing adjuvants and the proportions of adjuvants by adopting the common tablet production equipment under the condition that the disintegration time limit is guaranteed. The preparation method of the pharmaceutical composition comprises the steps: the aripiprazole is crushed and sieved for use, the adjuvants are weighed up based on the formula and mixed thoroughly to obtain adjuvant mixture; the aripiprazole is weighed up based on the formula and evenly mixed with the adjuvant mixture based on the principle of progressively adding in equal amount to make into a mixture; the pharmaceutical content of the mixture is determined, the weight of a tablet is calculated, a tablet is obtained by being pressed directly, and the hardness of medicine tablet is 8-10kg.
US8710045 Agents for preventing and treating disorders involving modulation of the ryanodine receptors The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.
US20080188438 Oligonucleotide molecule that interferes with the Fra-1/VEGF-D promoter or the Fra-1/c-Jun interaction to a subject suffering from a brain cancer Fra-1 serves as a target for diagnosing and treating glioblastoma multiforme and related brain cancers. Cancer in a brain tissue sample is detected by analyzing expression of Fra-1 in the sample. Brain cancer is treated by modulating Fra-1 gene expression in cells of the cancer, and by inhibiting angiogenesis associated with the cancer by interfering with Fra-1 binding to a VEGF-D promoter.
US7671199 dual inhibitor of VEGFR and FGFR tyrosine kinases; cancer The invention relates to an improved process for preparing [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula: Compound I has been shown to be useful for the treatment of certain types of cancer.
WO2007144422A2 Combination preparations comprising bifeprunox and l-dopa The invention concerns the use of a combination preparation of bifeprunox or its N-oxide, or pharmacologically acceptable salts of those compounds: and L-DOPA, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function, in particular Parkinson's disease and restless leg syndrome.
US8580761 Bispecific antisense oligonucleotides that inhibit IGFBP-2 and IGFBP-5 and methods of using same Bispecific antisense oligonucleotides which consist essentially of a sequence of bases that is complementary to portions of both the gene encoding human IGFBP-2 and the gene encoding human IGFBP-5 are useful in as antisense therapeutics in the treatment of endocrine-regulated cancers.
CA2186844C Use of serotonin antagonists (5ht3) for treating fibromyalgia 5-HT3 antagonists (e.g. tropisetron, ondansetron) are useful in the treatment of fibromyalgia.
US20090099137 Anti-Inflammatory Compounds and Uses Thereof Compounds of the general formula are disclosed with activity towards treating diseases related to inflammation, such as cancer, neurodegenerative and cardiovascular diseases. Pharmaceutical compositions and methods of use are also described.
US20120316125 Aminoglycosides: synthesis and use as antifungals The present invention relates to novel aminoglycoside analogs having certain substituents at the 6 position of ring III which exhibit improved antifungal activity but possess minimal antibacterial properties. The compounds of the present invention are analogues of kanamycin A. Also provided are methods of synthesizing and methods of using the compounds of the present invention. The compounds of the present invention are useful in treating or preventing fungal disease.
EP2780336A1 Structural variants of mycolactones for use in modulating inflammation, immunity and pain The present invention is related to variants of mycolactones of formula (I), processes for the preparation thereof, pharmaceutical compositions thereof and their use in modulating inflammation, immunity and pain. Y-O-W (I), wherein Y and W are as defined in claim 1.
CN101830884A Macrolide as well as preparation method and antibacterial application thereof The invention discloses macrolide as well as a preparation method and antibacterial application thereof. The macrolide has a structure shown as a formula (1) and is obtained by separating and identifying in gorgonian symbiotic bacterium Bacillus amyloliquefaciens SCSIO 00856 CCTCC NO: M 209257 fermentation liquor through column chromatography under normal pressure and one-dimensional and two-dimensional nuclear magnetic resonance spectroscopy. Through in vitro activity screening, the compound shown as the formula (1) is found to be capable of strongly suppressing the growth of strain Escherichia coli, Bacillus subtilis and Staphylococcus aureus, and the minimal inhibitory concentration of the compound is 0.1 microgram/ milliliter. The formula (1) is disclosed in the specification.
WO2013170968A1 Pharmaceutical composition comprising (1r,4r)-6'-fluoro-n,n-dimethyl-4-phenyl-4',9'-dihydro-3'h-spiro [cyclohexane-1,1'-pyrano-[3,4,b]indol]-4-amine and a salicylic acid component The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1 '-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is a salicylic acid component selected from the group consisting of acetylsalicylic acid, salicylic acid, salicylamide, ethenzamide, salsalate, dipyrocetyl, benorilate, diflunisal, guacetisal, and the physiologically acceptable salts thereof.
CN1969840A Plant extract for treating psoriasis The invention relates to the use of apple polyphenol in preparing medicaments or health products for the treatment and/or prevention of psoriasis pertaining to the field of pharmaceuticals or health products, wherein apple polyphenol obtained through industrialized production is used as the raw material. The pharmaceuticals and health products can be obtained through conventional preparing processes for for mass production at low cost.
CN102366437A Compound dexamethasone ointment and preparation method thereof The invention discloses a compound dexamethasone ointment and a preparation method thereof. The compound dexamethasone ointment is prepared from dexamethasone, camphor, menthol, and an emulsion substrate. The product provided by the invention is used for treating local pruritus, neurodermatitis, contact dermatitis, seborrheic dermatitis, and chronic eczema. Dexamethasone contained in the product is a glucocorticoid with functions of inflammation resisting and allergy resisting. Menthol and camphor provide functions of regional circulation promoting, and has mild functions of inflammation eliminating, pain relieving, and itching relieving.
US20100173015 Compositions and methods for the absorption, chelation, and elimination of trace elements This invention relates to compositions and methods effective for the absorption, chelation and elimination of trace elements, in particular tin, mercury, aluminium, cadmium, lead, and other metals, metaloids and lanthinides. It is comprised of dihydroquercetin and zeolite, with or without humic and fulvic acids. The combination acts as a powerful chelator and eliminator of toxic trace elements and enhances their absorption from the intestine, blood, and organs, and may be administered for the absorption, chelation and elimination of toxic or potentially toxic trace elements including metals and metalloids, and lanthinides.
CN1883306A Blood fat-lowering chewing tablet of housefly larvae chitooligosaccharides and method for making same Disclosed is a chitosan chewing tablet and its preparation method, wherein the tablet mainly comprises (by weight ratio) chitin oligosaccharide powder 10-30 parts, pre-gelatinized modified starch 20-40 parts.
EP1785136A2 Inhalation medicaments containing an anticholinesterase drug in conjunction with corticosteroid and betamimetic drugs An inhalable medicament (A) comprises a combination of 6beta ,7beta -epoxy-3beta -hydroxy-8-methyl-1alpha H,5alpha -H-tropanium salt 2,2-diphenylpropionate ester anticholinergic agent(s) (I) and EFGR kinase inhibitor(s) (II), optionally together with auxiliaries. An inhalable medicament (A) comprises a combination of tropane derivative anticholinergic agent(s) of formula (I), corticosteroid(s) (II) and beta -mimetic agent(s) (III) (optionally in the form of enantiomers, enantiomer mixtures or racemates, or solvates or hydrates), optionally together with pharmaceutical auxiliaries. [Image] X->monovalent anion, preferably chloride, bromide, iodide, sulfate, phosphate, methanesulfonate, nitrate, maleate, acetate, citrate, fumarate, tartrate, oxalate, succinate, benzoate or p-toluenesulfonate. - ACTIVITY : Antiinflammatory; antiasthmatic; antiallergic. - MECHANISM OF ACTION : Anticholinergic; beta -mimetic.
CN101659640B Ozagrel tromethamine, compound, preparation method and application thereof The invention provides an ozagrel salt which is stable, has functions of inhibiting platelet aggregation and removing blood-vessel convulsion, has good water solubility, and is prepared into a compound suitable for clinical application. The new compound is ozagrel tromethamine; and the ozagrel and the tromethamine are prepared by reaction in a solvent. The compound has good water solubility, strong and long-term stability, and the functions of inhibiting platelet aggregation and removing blood-vessel convulsion.
CN1883466A Preparation process of paclitaxel injection The invention relates to an injection of Paclitaxel, wherein specific auxiliary solvent is employed to increase the solubility of Paclitaxel and lower the toxic and side effects of Paclitaxel preparations, the bioavailability of the medicament can be improved, and the patient's tolerance can be enhanced.
WO2009046371A1 Methods of treating metabolic diseases This invention provides methods of treating metabolic disesases by administering a compound of Formula (I).
EP1492769B1 Novel process for the preparation of 1-phenyl-2-(2-pyridyl)ethanamine The invention relates to a novel process for the preparation of certain pharmaceutically active pyridyl compounds.
CN101100463A Benzofuran derivative and application thereof A 2-(6-hydroxy-2', 3'-dimethoxy-phenyl)-6-hydroxy-methoxy-Benfuran derivative is separated from (Lespedeza virgata(Thurb)DC), molecular formula is C17H1606, molecular weight is 316, it yellow green irregular powders. It has anti-oxidation function and can be used to treat nephritis.
WO2008077618A1 Use of xanthohumol and/or isoxanthohumol as an agent for preventing and/or combating liver diseases The present invention relates to the use of xanthohumol with formula (I) as an agent for the production of a preparation for preventing and/or combating liver diseases.
CN1872050A Drop pills of silymarin, and preparation method A dripping pill of silymarin for treating chronic metastatic hepatitis features high natural level and safety and low toxic by-effect. Its preparing process is also disclosed.
CN103340894A Preparation method of capsule capable of enhancing bone density The invention relates to a preparation method of a capsule capable of enhancing bone density. The capsule capable of enhancing bone density is obtained by the steps of taking any ingredient of a formula, mixing the ingredient with vitamin D, grinding to uniform, adding residual ingredients, mixing, pelletizing the mixture, drying, adding a proper amount of auxiliary materials, mixing uniformly, loading into capsules, carrying out quality detection and packaging. The capsule has a function of enhancing bone density, can prevent rachitis, tetany and chondropathy, is convenient for use, is a clinically popular, safe, stable and effective health-care product, and is an ideal product for modern pharmaceutical companies.
US7638538 4-chloro-N-({5-[({2-[(2-{[3-chloro-5-(trifluoromethyl)pyridin-2-yl]amino}ethyl)amino]-2-oxoethyl}amino)sulfonyl]thien-2-yl}methyl)benzamide; inhibitor of jun N-terminal kinase 2 and 33 inhibitor; autoimmune disorders The present invention is related to sulfonyl amino acid derivatives of formula (I), notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl amino acid derivatives. Said sulfonyl amino acid are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 33. The present invention is furthermore related to novel sulfonyl amino acid derivatives as well as to methods of their preparation.
WO2007132710A1 Bactericidal/preservative agent The object is to provide a bactericidal/preservative agent whose bactericidal/preservative ingredient is hardly degraded even when exposed to an environmental light such as an artificial light and natural light, and also provide use of the bactericidal/preservative agent. Provided is a bactericidal/preservative agent comprising a specific cyanin dye as a bactericidal/preservative ingredient and rutin or a sugar derivative thereof as an ingredient for improving the light resistance of the cyanin dye. Also provided is an agent for external application to the skin, which comprises the bactericidal/preservative agent.
US7423022 Nucleic acids for inhibiting hairless protein expression and methods of use thereof The present invention provides DNAzymes and ribozymes that specifically cleave Hairless Protein mRNA. The present invention also provides antisense oligonucleotides that specifically inhibit translation of Hairless Protein mRNA. The invention also provides various methods of inhibiting the expression of Hairless Protein. Finally the invention provides pharmaceutical compositions containing the instant DNAzymes, ribozymes and antisense oligonucleotides as active ingredients.
WO2010104035A1 Method for predicting therapeutic efficacy of chemotherapy on non-small-cell lung cancer Disclosed is an anti-tumor agent comprising tegafur, gimeracil, oteracil potassium and carboplatin, which is characterized by being administered to a patient who is selected by employing the level of thymidylate synthase as a measure.
US20050154047 Exert the beneficial effects of melatonin including anti-oxidation, sedation, anesthesia, protection of organs to chemical, infectious and cardiovascular damage, and can be administered in a water-based vehicle Disclosed are compounds that can serve as melatonin analogue prodrugs and that are soluble in aqueous solvents. Melatonin or melatonin analogues having modifications to the indole moiety are coupled to a tertiary amine to form a quaternary amine such that there is a saturated two-carbon linkage between the carbonyl of the melatonin structure and the amine nitrogen. This structure is stable in acidic environments, but is unstable at basic or neutral pH. Therefore, these melatonin analogue prodrugs are stable in a vial at acidic pH, but will breakdown upon injection into the body to liberate the melatonin analogue and the tertiary amine, which is nontoxic. The melatonin analogue being not modified on the indole moiety exerts similar pharmacological properties as melatonin: antioxidation, sedation and anesthesia.
US20080207565 Use of bisphosphonates for pain treatment A method for the treatment of pain, in particular antinociceptive or anti-allodynic treatment of pain, in a patient in need of such treatment, e.g. a patient with osteoporosis or osteopenia, a tumour patient or a patient suffering from an inflammatory disease, which comprises administering an effective amount of a bisphosphonate, e.g. zoledronic acid or salts or hydrates thereof, to the patient
CN1843369A Pharmaceutical composition soft capsule and its preparation method The invention relates to a pharmaceutical composition soft capsule preparation and preparation method, wherein the preparation is prepared from active components and contents selected from Kelarmycin, deflocculating agent, auxiliary solvent, solubilizing agent, suspension auxiliary agent and surface active agent through conventional methods.
CN102133215B Application of butylphenyl phthaleine in preparing medicament for treating chronic alcoholism The invention relates to a butylphenyl phthaleine, a medical salt thereof or an application of a medical compound which contains any one of the butylphenyl phthaleine and the medical salt thereof in preparing a medicament for preventing or treating chronic alcoholism. The medicament or medical compound is characterized by being efficient, harmless and free from addiction in the application of preventing or treating the chronic alcoholism.
CN1785008A Method for preparing milk powder contg. micron ginseng, antler, pearl and pollen pini for tonifying-Yang, dispelling-fatigue and enriching-calcium A micron-class health-care milk powder for invigorating Yang, relieving fatigue and supplementing Ca is prepared from traditional milk powder, micron-particles of ginseng, antler, pine pollen and pear, and oligose through proportional mixing, processing and fermenting. Its advantages are high effect and rich nutrients including vitamins, minerals, etc.
EP1942093A1 Novel cyclohexenone compounds from antrodia camphorata and application thereof The present invention relates to a novel compound and its uses, which is an extract isolated and purified from Antrodia camphorata, in particular to 4-hydroxy-2,3-dimethoxy-6-methy-5(3,7,11-trimethyl-dodeca-2,6,10-trienyl)-cyclohex-2-enone, and its use in tumor growth inhibition. The compound of the invention, which has never been discovered in Antrodia camphorata, can be applied in inhibiting the growth of cancer cells, such as breast cancer, hepatic cancer and prostate cancer; and be used as a pharmaceutical composition to inhibit the tumor growth; or further be applied in prevention of heart and blood vessel disease or dietary supplements for health needs through its antioxidant activity.
CN102603544A Anti-inflammatory compound, preparation and use thereof The invention relates to the fields of pharmaceutical chemistry and pharmacology, particularly to an anti-inflammatory compound (I), a preparation method and use of the anti-inflammatory compound. The pharmacological test proves that the compound (I) disclosed by the invention has a certain inhibiting effect on an inflammatory response caused by LPS (lipopolysaccharides), so that the compound can be used to treat septicopyemia and relevant inflammatory diseases.
US20120129903 Polymorphic, crystalline and mesophase forms of sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-ylthio) acetate, and uses thereof Crystalline polymorphs and solid mesophase forms of sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate are described. In addition, pharmaceutical compositions and uses of such compositions for the treatment of a variety of diseases and conditions are provided.
US20090117054 Sublingual spray for the treatment of pain This invention relates to a spray for sublingual administration, used in the treatment and management of pain, especially acute pain. Also provided are methods of treatment and management of pain, a metered dosage system for administration of the spray, and combination therapies.
WO2008012031A2 Blockers of gsk3 for the prevention and treatment of pemphigus vulgaris The invention relates to a method of preventing and treating pemphigus vulgaris comprising administering a GSK3 blocker, and the use of such blockers in said prevention and treatment and in the manufacture of medicaments for preventing and treating pemphigus vulgaris. In particular the invention relates to a method of preventing and treating pemphigus vulgaris comprising administering a GSK3β blocker, and the use of such blockers in said prevention and treatment and in the manufacture of medicaments for preventing and treating pemphigus vulgaris. Preferred is the use of GSK3β blockers which are selective for GSK3β, i.e. which selectively reduce enzyme activity of GSK3β but not to a reasonable extent of GSK3α.
US20120265119 Transdermal Delivery of Medicinal Cetylated Fatty Esters using Phonophoresis or Iontophoresis The use of phonophoresis or iontophoresis to enhance transdermal delivery of medicinal Cetylated fatty esters when applied in cream or gel compositions is disclosed. These compositions provide hydrophilic salt forms and penetration-enhancing vehicles that work in conjunction with phonophoresis or iontophoresis to increase the efficacy of the medicinal actives.
WO2010030967A1 4-aryloxyquinolin-2(1h)-ones as mtor kinase and pi3 kinase inhibitors, for use as anti-cancer agents 4-aryloxyquinolin-2(1H)-ones as mtor kinase and PI3 kinase inhibitors, for use as anti-cancer agents. Compounds of the formula I and pharmaceutically acceptable salts thereof, wherein A, B, R1, R2, R3, R4, R5, R6, and R7 are defined as set forth herein are disclosed. Also disclosed are pharmaceutical compositions comprising the compounds of the invention and a pharmaceutically acceptable carrier, methods of making the compounds of the invention and methods of using the compounds for inhibiting mTOR and PI3 kinases and for treating cancers.
EP1577322A1 Novel proteins and use thereof Compounds that inhibit the expression of a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 4, SEQ ID NO: 7 or SEQ ID NO: 10 or the expression of a gene for the protein, the antisense polynucleotide comprising the entire or part of a base sequence complementary or substantially complementary to DNA encoding the protein or its partial peptide, the antibody to the protein or its partial peptide, etc. are useful as prophylactic/therapeutic agents for cancer, etc., apoptosis promoters, etc.
US20120082706 Medical device for drug delivery A medical device for safe and sure delivery of drugs to the lesion and a method for production thereof. The medical device has at least part of its surface in contact with the lumen wall tissue of the living body coated with a drug releasing layer containing a drug and a phospholipid, the drug and the phospholipid forming a solid dispersion.
CN103720710A Pharmaceutical composition capable of increasing bone density and preparation method of pharmaceutical composition The invention discloses a pharmaceutical composition capable of increasing bone density. The pharmaceutical composition is prepared from the following raw materials in parts by weight: 150-350 parts of calcium carbonate, 100-250 parts of D-glucosamine hydrochloride and 0.2-0.6 part of vitamin D. The pharmaceutical composition, for reasons of osteoporosis, can prevent bone loss and increase bone density through methods of supplementing calcium, repairing cartilage injury and protecting bone joint; the pharmaceutical composition can be used for preventing and controlling osteoarthritis and osteoporosis.
EP1781271A1 Arylidenes for the treatment of estrogen related receptor-alpha mediated diseases Therapeutic methods of using certain heterocyclic arylidene aryl ether compounds for treating diseases or disorders mediated through modulation of estrogen related receptor alpha are described.
US7572888 Fusion protein comprising arrestin and green fluorescent protein for use in identifying ligands for g-protein coupled receptors Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process. Constructs useful in such methods are described.
WO2008067280A3 Combination of iap inhibitors and flt3 inhibitors The present invention relates to combinations of IAP inhibitors and FLT3 inhibitors, pharmacological compositions comprising said combination, methods of treating hematological malignancies, including acute myeloid leukemia (AML), comprising the combination of a compound that inhibits the binding of the second mitochondria-derived activator of caspase (Smac) protein to inhibitor of apoptosis (IAPs) (IAP inhibitor) and one or more pharmaceutically active agents and the use of these combinations for the treatment of acute myeloid leukemia; and a commercial package comprising said combination.
CN101270078A Metallic supermolecule compound for inhibiting telomere enzymatic activity, using method and uses thereof The present invention relates to a metal supramolecular compound that can be used for inhibiting the activity of telomerase, a method and an application thereof. The metal supramolecular compound has a structure as shown in the formula I; wherein, the formula III is Ni<2+> or Fe<2+>; the molecular formula of ligand is C25H20N4; and the ligand has a structure as shown in II. The metal supramolecular compound comprises a pair of isomers with corresponding structures, P and M. The metal supramolecular compound can inhibit the proliferation of the active cells of the telomerase, such as the proliferation of tumor cells, and can induce the aging of the tumor cells. So the metal supramolecular compound that can be used for inhibiting the activity of the telomerase can be used for preparing antineoplastics.
US20090110646 Product for Treating the Skin and Mucous Membranes, and Relative Method of Preparation A method for preparing a product for treating the skin and mucous membranes comprises the steps of making available a suitable quantity of trichloracetic acid, making available a suitable quantity of hydrogen peroxide, making a first mixture of the trichloracetic acid and the hydrogen peroxide, making available a determinate quantity of the basic compound able to achieve a buffer effect of the trichloracetic acid comprised in the first mixture, and adding the basic compound.
US7094784 High affinity ligands for nociceptin receptor ORL-1 Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.
CN101730684A sulfonyl-quinoline derivatives New mGluRl and mGluR5 receptor subtype preferring ligands of formula: (I) and/or salts and/or hydrates and/or solvates thereof, to the processes and intermediates for their preparation, to pharmaceutical compositions containing these compounds and to their use in therapy and/or prevention of a condition which requires modulation of mGluRl and mGluR5 receptors.FORMULE (I) wherein Ar1 represents anoptionally substituted phenyl or heteroaryl group; Ar2 represents a substituted phenyl or an optionally substituted heteroaryl group; R1, R2, R3 and R4 represent independently a substituent selected from hydrogen, halogen, cyano, alkyl, alkoxy, hydroxy, trifluoromethyl, amino, alkylamino, dialkylamino, aminomethyl, alkylaminomethyl, dialkylaminomethyl.
WO2010108268A1 Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.
CN102641273A New application of asiatic acid and derivatives thereof The invention relates to a new application of asiatic acid and derivatives thereof, and particularly relates to an application of asiatic acid and derivatives thereof in the preparation of medicaments for prevention and/or treatment of breast-related diseases, or breast health-care products. Studies confirm that both oral administration and external use of asiatic acid and derivatives thereof have significant inhibition effect on breast hyperplasia of experimental rats.
US20100152164 Method For Stabilizing Anti-Dementia Drug The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug.
CN103709138A 5-(fluoroquinolone C3- methylene)3-pyrrolic amide derivative as well as preparation method and application thereof The invention discloses a 5-(fluoroquinolone C3- methylene)3-pyrrolic amide derivative as well as a preparation method and application thereof, belonging to the technical field of medicines. A chemical structural formula of the 5-(fluoroquinolone C3-forked methyl)3-pyrrolic amide derivative is as shown in formula I: FORMULA I. The 5-(fluoroquinolone C3- methylene)3-pyrrolic amide derivative has stronger in-vitro cytotoxic effect on human hepatocellular carcinoma cells and leukemia cancer cell line, has stronger antitumor activity and can be prepared into an antitumor drug by salifying acid which is acceptable by human body or mixing with a medicinal carrier.
WO2012028965A3 Combination of semax and choline alfoscerate with antihypoxic neuroprotective, and antiαμνesic action and with ability to improve physical efficiency This invention relates to medicines, in particular, to pharmaceutical compositions which have an antihypoxic, neuroprotective, and antiamnesic action and an ability to improve physical efficiency and which are also used to treat acute and chronic cerebral-circulation disorders, including ischemic stroke and other diseases and conditions accompanied by a lower cognitive function. This pharmaceutical composition contains such active ingredients as Semax and choline alfoscerate at a ratio between 1 : 50 and 1: 8,000 (w/w), respectively, as well as pharmaceutically acceptable excipients. This invention solves such a problem as a product range extension for simple-composition drug products with a strong neuroprotective action accompanied by an antihypoxic and antiamnesic action and by an ability to improve physical efficiency.
CN101219212A Eatable face pack for beauty treatment skin-protection and technique of preparing the same The invention relates to an eatable facial mask for skin care, in particular to a skin care preparation made of a combination of garlic glucoside and fresh fish collagen, pawpaw, cucumber and other fruit and vegetable pastes. The invention is a pure food preparation with the functions of sterilizing, diminishing inflammation, antisepsis, antioxidation and clearing free radical of human cells. The preparation has sterilization and antisepsis effects, which is ensured not to be degenerative without the addition of chemical antiseptic agent or antistaling agent. The invention is an eatable skin care facial mask with health care effect on skin tendering, whitening, speckle removing and anti acne.
CN101402661A Uses of iridoid glycoside compounds in preparing hemostatic and pain easing medicament The invention provides the application of iridoid glycosides in the preparation of hemostasis and analgesia medicaments, in particular to the application of the iridoid glycosides, such as 8-O-acetyl shanzhiside methyl ester, 6-O-acetyl shanzhiside methyl ester, Penstemoside, acetyl shanzhiside methyl ester, loganin, Phloyoside II or 8-dehydroxystilbene shanzhiside and the like in the preparation of hemostasis and analgesia medicaments. The iridoid glycosides show good hemostasis, procoagulant and analgesia effect through the influence on bleeding time, capillary coagulation time in mice with tails cut and the influence on twisting times caused by injecting acetic acid in the abdominal cavityies mice. The iridoid glycosides is combined with dressing regularly used in medicine and pharmacology, and then prepared into any oral or parenteral agent by the regular method.
US20100226979 Taste Masked Phamaceutical Composition for Oral Solid Dosage form and Process for Preparing the Same Using Magnesium Aluminium Silicate Disclosed herein a taste masked pharmaceutical composition suitable for oral solid dosage form comprising adsorbate of unpleasant or objectionable tasting active pharmaceutical agents and water insoluble polymer, wherein said active is first blended with an adsorbent such as magnesium aluminium silicate to achieve partially or significantly taste masking of said active and further granulated the resultant blend with water insoluble polymer to strengthen the taste masking without affecting the release of said active.
US20110021499 Urethral suppositories for overactive bladder Urethral suppositories containing a mixed-activity anti-cholinergic drug and methods of use for treatment of over-active bladder are provided. Buffering drugs to pH near their pKas can result in a desired proportion of uncharged drug and can enhance absorption of the agents into urethral tissues.
CN103739652A New 23, 29-drop oleanolic acid compound, preparation method thereof and application in preparation of glucosidase inhibitor medicines The invention discloses new 2-hydroxy-3-carbonyl-23, 29-dinorolean-1, 4, 12, 20 (30)-tetraene-28-acid, a preparation method thereof and an application in preparation of glucosidase inhibitor medicines. An alpha-glucosidase inhibitor with strong effects is extracted and separated from an akebia plant, and plant sources are rich. Furthermore, when fruit extraction is performed, the plant can not be damaged and can be utilized for a long time, so that economic benefits are improved, and the environment-friendly effect is further achieved. Pharmacological experiments show that the in-vitro alpha-glucosidase inhibition activity of the compound, namely 2-hydroxy-3-carbonyl-23, 29-dinorolean-1, 4, 12, 20 (30)-tetraene-28-acid is about 5 times of that of a first-line diabetes medicine, namely acarbose, so that the compound is expected to be used for developing medicines for preventing and treating type II diabetes and has good application and development potentials.
US8343554 Formulations for the treatment of arthritis conditions The present invention relates to formulations comprising combinations of analgesic/anti-inflammatory, immunomodulating and cartilage-reconstructing agents in particular comprising saligenig, boswellic acid, procyanidins, N-acety-glucosamine and either glucoronic acid or glucoronolactone, for the treatment of rheumatoid arthritis and, more generally, of arthritis conditions.
WO2011051960A3 Process for producing rapamycin derivatives The invention relates to processes for the preparation of compound of CCI-779 having the Formula (I), which is useful as an antineoplastic agent. The invention further relates to certain novel intermediates useful in the preparation of compound of CCI-779 and processes for their preparation. The invention also relates to pharmaceutical compositions that include the compound of CCI-779, prepared according to the processes disclosed herein.
EP1887017A1 Prebiotic carbohydrate The invention relates to the use of a carbohydrate represented by the formula Galn-Xo-Galp, wherein n and p are integers in the range of 0-9, with the proviso that the sum of n and p is in the range of 1-9, o is an integer in the range of 1-9, with the proviso that the sum of n, o and p is 2-10, Gal is a galactose moiety, X0 represents a monosaccharide moiety different from Gal (if o=1) - which monosaccharide moiety is optionally an acetylated or reduced monosacharide moiety - or an oligosaccharide moiety (if o>1), comprising at least one monosaccharide moiety different from Gal - which monosaccharide moiety is optionally an acetylated or reduced monosacharide moiety - in the manufacture of a food or medicament for providing an effect in a distal part of the colon, in particular for stimulating beneficial bacteria in the distal part of the colon of a human, another mammal or another vertebrate.
US20090041857 Analgesic Cream A herbal topical composition is used having complexed trace minerals capable of effectively reducing bone and joint inflammation by inhibiting inflammation pathways and in particular COX-2. The herbal composition having trace elements in a topical carrier reduces inflammation while avoiding the side effects associated with traditional drug therapy.
CN101683357A Astragalus polyose solution for aquatic animals and preparation method thereof The invention relates to an astragalus polyose solution for aquatic animals and a preparation method thereof, belonging to the field of aquaculture industry, in particular to a Chinese and Western compound medicine. The preparation method comprises the following steps: adding 5-12 parts by weight of astragalus polyose and 5-10 parts by weight of lentinan into partially quantitative distilled waterwith the temperate of 100 DEG C; stirring till dissolving; cooling to normal temperature; regulating a pH value ranging from 6.0 to 8.0 by a conventional method; adding 0.5-3 parts by weight of colistin sulfate and the balance of the distilled water up to 100 parts by weight; uniformly stirring so as to obtain brown liquid; and canning according to packaging specifications so as to obtain a finished product of the astragalus polyose solution. The invention adopts the Chinese and Western compound medicine to be prepared into a solution formulation which can not only be used for oral administration and bait mixing, but also be directly splashed into a pond externally, thereby solving the problems of a background technology.
US20060154952 Pharmaceutical compositions comprising a combination of rapamycin or its derivative and pimecrolimus for the treatment of inflammation-and ummunologically-mediated diseases The present invention relates to pharmaceutical compositions comprising in combination rapamycin or a rapamycin derivative and a compound of formula I, e.g. useful for the treatment of inflammatory and immunologically-mediated diseases, including autoimmune diseases.
CN102552241A Application of formononetin in preparing medicine for preventing and treating airway inflammation and asthma The invention relates to a novel application of formononetin in the medical science, in particular to the application of formononetin in preparing medicine for preventing and treating airway inflammation and asthma. Pharmacological test result shows that the formononetin participates in reducing the allergic airway inflammation of model animals/occurring and developing of asthma lesion; reducing the of damage inflammatory factor to the human bronchial epithelial cell in vitro and the formononetin can be used for preparing the medicine for treating airway inflammation diseases, such as asthma, bronchitis, capillary bronchitis and air or non-air idiotoxin or inflammatory or non-inflammatory of irritant; and specifically, the formononetin has the application in preparing medicine for treating allergic airway inflammation and asthma disease.
US20060063944 Estrone derivatives and process for producing same A compound of formula (I) (where X1 and X2 represent independently a hydrogen atom or a group of formula (II) R1 represents a linear or branched halogenoalkyl group having 1-7 carbon atoms; Ra represents a hydroxyl group and Rb represents a linear or branched alkynyl group having 2-5 carbon atoms, or Ra and Rb, when taken together with the carbon to which they are bound, represent a carbonyl group; m is an integer of 2-14; n is an integer of 2-7; provided that X1 and X2 are not both a hydrogen atom), stereoisomers of the compound, or hydrates, salts or esters thereof, as well as a pharmaceutical composition containing a therapeutically effective amount of the compound.
WO2013175316A3 Dopaminergic modulators for the treatment of huntington's disease A method for treating Huntington's disease in a mammal in need thereof is disclosed. The method comprises administering to the mammal an effective amount of a compound of Structural Formula I, or a pharmaceutically acceptable salt thereof, having an averaged affinity for dopamine D2 receptors characterized by a Kd of about 10-5 to about 10-8 M, and an affinity for a pre-synaptic dopamine D2 receptor, as characterized by Kd, that is about 5 to about 100 times greater than the affinity of the compound for a post-synaptic dopamine D2 receptor, as characterized by Kd.
WO2006117570A1 Quinoline derivatives as kinase enzyme inhibitors Compounds of formula (IA) or (IB) are inhibitors of aurora kinase activity, and are useful in the treatment of cell proliferation disease and other conditions associated with inappropriate aurora kinase activity wherein R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, -C(=O)-, -S(=O)2-, -C(=O)O-, -C(=O)NR3-, -C(=S)-NR3, -C(=NH)-NR3 or -S(=O)2NR3- wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 and L2 are linker radicals as defined in the claims; X1 represents a bond, -NR4C(=O)-, -C(=O)NR4-, -NR4C(=O)-NR5-, -NR4S(=O)2-, or -S(=O)2NR4- wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; -C(=O)-; or -S(=O)2-; z is 0 or 1 R4 is C1-C4 alkoxy, hydrogen or halo; r and s are independently 0 or 1 ; and rings A, B and C are mono- or bi-cyclic carbocyclic or heterocyclic rings or ring systems having up to 12 ring atoms.
EP1790653A2 Novel polymorphic form of 17-beta-(n-ter.butyl carbamoyl)-4-aza-5-alpha-androst-1-en-3-one and a process for preparing it The present invention relates to a novel polymorphic form of 17-β-(N-Ter.Butyl Carbamoyl)-4-aza-5-α-androst-1-en-one (Finesteride) and processes for preparing the form.
WO2014101295A3 Isoxazole derivative that inhibits activity of janus kinases (jaks) Disclosed is an isoxazole derivative that inhibits the activity of the Janus kinases (JAKs), the structure thereof as presented in formula I, formula II, formula IX, and formula XI. The substituent groups in the formulas are described in the description. Also disclosed are the pharmaceutical composition of the compound and a related use in medicine preparation.
WO2006075020A2 Ampa antagonist for the treatment of dizziness, including vertigo and meniere's disorder The invention relates to the use of 8,9-dimethyl-5-phenyl-11 H-1 ,3-dioxolo[4,5-h]-imidazo[1 ,2-c][2,3]benzodiazepine: tautomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of this compound and its tautomers and N-oxides, for the preparation of a pharmaceutical composition for the treatment, amelioration or prevention of dizziness, including vertigo and Meniere's disorder.
WO2007143951A1 COMPOUNDS WITH THE ACTIVITY OF PPARγ AGONIST AND APPLICATION THEREOF Compounds of the said formula (I) or salts thereof, their preparation and the application for the treatment of the diseases associated with PPARγ receptor thereof are disclosed, wherein the groups of formula (I) as shown in the description. The said compounds with the activity of specially agitating PPARγ are selective PPARγ agonist and can be used for the treatment of the diseases associated with PPARγ receptor, as well as that associated with blood sugar singularly rising, especially such as diabetes or metabolic syndrome etc.
US6887501 Isolated from cocoa beans; solvent extraction; nitric oxide synthase/lipoxygenase/cyclooxygenase modulators The present invention is directed to a method of processing a fat-containing bean, e.g., cocoa beans, for producing solids comprising active polyphenols and/or fat-containing products, comprising extracting the fat to produce solids and fat-containing products. Additionally, the inventive method also provides cocoa compositions comprising at least one active polyphenol, wherein the concentration of the polyphenol(s) with respect to the nonfat solids is conserved with respect to the concentration of the active polyphenol(s) in the bean from which the compositions are derived.
WO2005066181A1 Process for the preparation of 1,3-dioxolo [4,5-c] piperidin-7-ols and related compounds A process is disclosed for preparation of piperidine derivatives, preferably 1,3-dioxolo 4,5-c piperidin-7-ols such as (3aS, 4R, 7S, 7aR)-2,2,4-trimethyl-1,3-dioxolo 4,5-c piperidin-7-ol and its polyhydroxylated derivatives. In a preferred process, 2,3-O-isopropylidene-1,4-lactone (A) is reacted with methanesulfonyl chloride to form (3aR, 4S, 6aR) methanesulfonic acid 2,2-dimethyl-6-oxo-tetrahydro-furo 3,4-d 1,3 dioxol-4-ylmethyl (B). Compound (B) is then reacted with methylmagnesium halide to form (3aR, 4S, 6aR)-methanesulfonic acid 6-hydroxy-2,2,6-trimethyl-tetrahydro-furo[3,4-d][1,3]dioxol-4-ylmethyl ester (C), which is reacted with phthalimide to form (3aR, 4S, 6aR)-2-(6-hydroxy-2,2,6-trimethyl-tetrahydro-furo[3,4-d][1,3]dioxol-4-ylmethyl)-isoindole-1,3-dione (D). Compound (D) is reacted with hydrazine to form (3S, 7S, 7aR)-2,2,4-trimethyl-3a,6,7,7a-tetrahydro- 1,3 dioxolo 4,5-c pyridin-7-ol (E), which is hydrogenated to give the corresponding 1,3-dioxolo 4,5-c piperidin-7-ol (F). The synthesis has an overall yield which is typically greater than 50% and avoids the use of reagents such as triflic anhydride and sodium azide.
CN103589422A Preparation method of fluorescent nanoparticles for suppressing cancer cell The invention relates to a preparation method of novel fluorescent nanoparticles. The novel fluorescent nanoparticles (PIOT-HA) are prepared by the interaction of cationic polyester (PIOT) and anionic hyaluronic acid (HA) in water solution, and can eliminate latent toxicity and carcinogenic risk while keeping fluorescence property of conjugated polymer. Under white light, the PIOT-HA nanoparticles can activate oxygen to generate reactive oxide species (ROS), which can deactivate CD44 proteins and effectively suppress metastasis of MDA-MB-231 cancer cells. Therefore, the PIOT-HA nanoparticles have good application prospect in cancer treatment.
WO2011086412A3 Imidazolone-chalcone derivatives as potential anticancer agent and process for the preparation thereof The present invention provides Chalcone linked Imidazolone compounds of formula (A) A as anti cancer agent against fifty three human cancer cell lines, Formula (I), wherein R = H, OMe, R1 = H, CI, F, OH, OMe, R2 = H, OH, OMe, R3 = H, OMe, CH3, R4 = H, CI, F, OH, OMe, CH3, R5 = H, OMe, CH3.
CN102783647A Preparation method of kudzu root isoflavone powder The invention discloses a preparation method of kudzu root isoflavone powder. The preparation method of the kudzu root isoflavone powder includes: using kudzu roots as raw materials, drying, smashing, adding ethanol, then adding cellulose and protease to perform enzymolysis, decompressing and concentrating, and freezing and drying to obtain kudzu root isoflavone; mixing the kudzu root isoflavone, beta-cyclodextrin and soybean lecithin, adding water to make 1000mL kudzu root isoflavone emulsion, and performing ultrasonic processing for 20 minutes; atomizing the kudzu root isoflavone emulsion which is processed by ultrasonic into liquid drops through a spray gun, freezing and curing rapidly after the liquid drops are contacted with compressed nitrogen, placing cured samples in a vacuum freeze drying apparatus to be dried, and obtaining the kudzu root isoflavone powder. The kudzu root powder manufactured by the method fills the blank that no kudzu root powder exists on the domestic market, enzyme treatment is matched with digestion so as to extract flavonoid materials effectively, processing steps are reduced, efficiency is improved, kudzu root flavone can be kept maximally by using a spray freeze drying technique, and products with high economic value and health care value can be obtained.
US7163808 Method for selectively delivering agent to arterial smooth muscle cells in mammal comprising administering agent and substance which selectively binds arterial smooth muscle cell-specific surface molecule selected from ephrin family Arterial and venous smooth muscle cells are molecularly distinct from the earliest stages of angiogenesis through to adulthood. This distinction is revealed by expression on arterial cells (e.g., arterial endothelial cells, arterial smooth muscle cells) of a transmembrane ligand, called EphrinB2 whose receptor EphB4 is expressed on venous cells. Targeted disruption of the EphrinB2 gene prevents the remodeling of veins from a capillary plexus into properly branched structures. Moreover, it also disrupts the remodeling of arteries, suggesting that reciprocal interactions between pre-specified arterial and venous cells are necessary for angiogenesis. Expression of EphrinB2 in arterial cells (e.g., arterial endothelial cells, arterial smooth muscle cells) can be used to advantage in methods for targeting agents and/or encoded polypeptides to arterial smooth muscle cells, altering angiogenesis, assessing the effect of agents on arterial smooth muscle cells, identifying arterial smooth muscle cells, isolating arterial smooth muscle cells and production of artificial vessels, for example.
US7807167 using an agent that specifically binds to an alpha-4 integrin or a dimer comprising an alpha-4 integrin; treatment of multiple sclerosis or inflammatory disease of the gastrointestinal tract A method of chronically reducing a patient's pathological inflammation via the administration of an agent that specifically binds to an alpha-4 integrin or a dimer comprising an alpha-4 integrin is disclosed. The agent provided must have a binding affinity such that administration is sufficient to suppress pathological inflammation, and the agent is administered chronically to provide long-term suppression of pathological inflammation.
CN1615871A Gatifloxacin intra-venous trans fusion preparation and its preapring method The intravenous Gatifloxacin transfusion preparation is freeze dried Gatifloxacin powder preparation or glucose injecta of Gatifloxacin. The preparation process includes the following steps: weighing Gatifloxacin in recipe amount and optional supplementary material, adding partial injection water and pharmaceutically acceptable acid, and stirring to dissolve; regulating pH with pharmaceutically acceptable alkali to 3.5-6.0; adding supplementary material in recipe amount, stirring to dissolve, adding injection water to full amount, adding active carbon 0.05-0.5 wt%, stirring for 20 min, eliminating carbon with 5 micron titanium rod, fine filtering with tubular filter of 0.45 micron and 0.22 micron micropore filtering film and packing; and freeze drying to prepare freeze dried preparation or directly packing and sterilizing to prepare glucose injection.
EP2001454A2 Use of at least one cytosolic phospholipase a2 inhibitor as a medicine for symptomatic treatment of mucoviscidosis The purpose of this invention is the use of at least one cytosolic phospholipase A2 (cPLA2) inhibitor in the preparation of a medicine intended for preventive and/or remedial symptomatic treatment of mucoviscidosis, and particularly the increased secretion of mucus in mucoviscidosis.
CN102675346A Levamisole organic acid salt, synthetic method for levamisole organic acid salt and medicinal composition of levamisole organic acid salt The invention relates to levamisole organic acid salt, a synthetic method for the levamisole organic acid salt and a medicinal composition of the levamisole organic acid salt. The levamisole organic acid salt is represented by a general formula (I). The synthetic method for the levamisole organic acid salt comprises the following steps of: dripping an aqueous solution of sodium hydroxide into levamisole hydrochloride which is taken as an initial raw material, reacting for a period of time, extracting by using an organic solvent, and drying and concentrating to obtain white solid levamisole free alkali; and dissolving the levamisole free alkali into a reaction solvent, adding organic acid at certain temperature, reacting under stirring, filtering, freezing a filtrate till the temperature of 2 to 10 DEG C, slowly dripping a precipitation solvent under stirring, precipitating crystals, filtering, washing, and drying to obtain the levamisole organic acid salt. The method is simple and quick and is short in production cycle, low in cost and high in yield, and reaction conditions are mild. The levamisole organic acid salt has high water solubility, stability and bioavailability. The medicinal composition contains a therapeutically effective amount of levamisole organic acid salt shown as the formula (I) and a pharmaceutically acceptable carrier.
CN103417962A Pharmaceutical preparation for treating viral pneumonia or viral cold, and preparation method and application thereof The invention relates to a pharmaceutical preparation for treating and/or preventing viral pneumonia or a viral cold caused by avian influenza, and a preparation method and the application thereof. With the unexpected combination of conventional drugs, the pharmaceutical preparation has an excellent effect on treating and/or preventing the avian influenza, particularly avian influenza patients, can effectively prevent and treat the viral pneumonia caused by avian influenza viruses, prevents the cross infection and the transmission of the avian influenza among humans, and has good effects on disease prevention and treatment.
CN102058611A Compound solid preparation for treating asthma The invention relates to a compound solid preparation for treating asthma, which consists of ambroxol hydrochloride and azithromycin which serve as active ingredients and auxiliary materials, wherein the ratio of the ambroxol hydrochloride to the azithromycin is 2:1-10:1, the weight ratio of the active ingredients to the auxiliary materials is 1:5-100, and preferably the medicament content of each single dose is 7.5:2 to 30:12 mg. The oral solid preparation containing the ambroxol hydrochloride and the azithromycin which serve as the active ingredients has the characteristics of stability in storage, convenience for carrying, capability of reducing production cost, and suitability for large-scale production. The oral solid preparation has the obvious synergistic effect on the relief of symptoms such as dyspnea and the like caused by airway obstructive diseases such as bronchial asthma, chronic bronchitis, emphysema and the like.
CN103405730A Cold injury treatment liquid and preparation method thereof The invention provides a cold injury treatment liquid. The cold injury treatment liquid is prepared from the following medicines in parts by weight: 1-2 parts of ligusticum wallichii, 1-2 parts of aizoon stonecrop herb, 1-2 parts of gynura segetum, 4-6 parts of angelica sinensis, 2-3 parts of dried ginger, 2-3 parts of pepper, 2-6 parts of notopterygium root, 3-5 parts of schizonepetae herba, 1-2 parts of radix sileris, 4-8 parts of fennel, 4-6 parts of cinnamon, 3-5 parts of radix angelicae, 1-3 parts of camphor and 100-200 parts of 75% medical alcohol. The cold injury treatment liquid has the advantages of washing, removing stains and having functions of skin moistening and protection, sterilization and itching relieving, scurf removal and peculiar smell removal and prevention and adjuvant therapy effects on skin diseases, skin itches, certain gynecological diseases and venereal diseases.
WO2005103014A1 2,4-dioxo-5-(2-hydroxy-3,5-dichloro-benzylidene)imino-1,3-pyrimidine salts The invention relates to medicine, in particular to pharmacology, more specifically to synthetic active pyrimidine derivatives. The inventive 2,4-dioxo-5-(2-hydroxy-3,5-dichloro-benzylidene)imino-1,3-pyrimidine salts of general formula (I), wherein X is selected from a Na, K, NH4 + group which exhibits a biological activity substantially are directed against different fungus, bacteria and viruses and usable for this purpose in veterinary science, cosmetology, building construction, the food, leather, wood-working and other industries.
US20120292797 Solid pharmaceutical dispersions with enhanced bioavailability Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.
CN102085186B Glycyrrhetinic acid emulsion and preparation method thereof The invention relates to glycyrrhetinic acid emulsion and a preparation method thereof, and the emulsion contains glycyrrhetinic acid, oil, an emulsifier and a stabilizer, wherein the weight-volume percent of the glycyrrhetinic acid is 0.6-2%, the weight-volume percent of the oil is 5-30%, the weight-volume percent of the emulsifier is 0.1-6%, and the weight-volume percent of the stabilizer is 0.01-3%. The structure of the glycyrrhetinic acid does not need to be transformed, thereby keeping the original efficacy; simultaneously, the use of an organic solvent can be avoided, the potential safety hazard can be reduced, and the industrial production can be facilitated.
US6974828 3-((2-((3-((Amino(imino)methyl)amino)benzoyl)amino)phenyl)sulf anyl)- 3-(3-pyridinyl)propanoic acid, for example; angiogenic inhibitors; antitumor, -carcinogenic, -metastatic, -diabetic, -arthritic and inflammatory agents; bone disorders Novel propanoic acid derivatives are integrin receptor antagonists or inhibitors, in particular of the avb3 integrin receptor. The compounds of the invention are for instance useful for the treatment of solid tumors by inhibition of angiogenic growth of tumor vessel network, thus promoting tumor regression, inhibition of metastatic spread, thus avoiding cancer metastases, inhibition of bone resorption, thus controlling osteoporosis, inhibition of smooth muscle cells migration into neointima, thus blocking restenosis after percutaneous coronary angioplasty and the treatment of other pathological conditions mediated by cell adhesion, cell migration or angiogenesis such e.g. diabetic retinopaty, rheumatoid arthritis and inflammation.
WO2008022807A2 Lipoxin a4 analogs for the treatment and prevention of intestinal fibrosis This invention relates to the use of lipoxin A4 analogs as therapeutic agents in the treatment and/or prevention of intestinal fibrosis.
CN102584799A Aromatic nitrogenous six-membered ring compounds An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R<1> is a substituted or unsubstituted lower alkyl group, -NH-Q-R<3> (R<3> is a selectively substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or -NH-R<4> (R<4> is a substituted or unsubstituted cycloalkyl group); R<2> is a substituted or unsubstituted aryl group; one of Y and Z is =CH-, and the other is =N-, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.
CN101367810A Novel carbpenem antibiotic The present invention belongs to the technical field of medicine, in particular to a novel carbapenem antibiotic shown in the formula (I) and a pharmaceutically acceptable salt, an easily hydrolyzed ester, an isomer, a hydrate and a hydrate of the ester or the salt thereof: wherein, R<1>, R<2>, R<3>, R<4> and R<5> are defined in the description. The present invention also relates to preparation methods of the compounds, drug combinations and applications of the compounds in the preparation of drugs for treating and/or preventing infective diseases.
CN101365476A Combined use of dpp iv inhibitors and gastrin compounds The invention relates to compositions, conjugates, and methods for the prevention and/or treatment of a condition and/or disease comprising a therapeutically effective amount of a DPP-IV inhibitor and a gastrin compound. The combination of a DPP-IV inhibitor and a gastrin compound provides beneficial effects, in particular sustained beneficial effects, in the prevention and/or treatment of conditions and/or diseases for which either a DPP-IV inhibitor or a gastrin compound have been demonstrated to have a therapeutic effect, including but not limited to diabetes, hypertension, chronic heart failure, fluid retentive states, obesity, metabolic syndrome and related diseases and disorders. Combinations of a DPP-IV inhibitor and a gastrin compound can be selected to provide unexpectedly additive effects or synergistic effects.
WO2014153226A1 Arginine methyltransferase inhibitors and uses thereof Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
CN101270122A Amino acid norcantharidin acid imide derivative with optical activity and preparation method thereof The present invention discloses an optically active amino acid norcantharidinimide derivant and a preparation method thereof, L-amino acid and norcantharidin are resolved in alcohol or alcohol / water system, the produced solution is heated and reflowed in order to obtain reaction solution, which is then condensed and added with organic solvent for crystallization, and after the reaction solution statically cools down, the optically active L-amino acid norcantharidinimide derivant is obtained. The optically active amino acid norcantharidinimide derivant provided by the present invention has good inhibitory activity against the cancer cell lines of the human body. The preparation method has the advantages of simplicity and high yield and purity of products.
US20100144832 Prostate Cancer-Specific Alternations in ERG Gene Expression and Detection and Treatment Methods Based on Those Alterations The disclosure describes alterations in ERG gene expression. ERG isoforms and promoter sequence of the ERG gene that are involved in, or associated with, prostate cancer are provided. The disclosure further provides therapeutic compositions and methods of detecting, diagnosing, prognosing, and treating prostate cancer, including biomarkers for detecting the expression of two or more of the following genes: PSA/KLK3, PMEPA1, NKX3.1, ODC1, AMD1, and ERG.
CN102670537A Trimetazidine dihydrochloride sustained release tablet and preparation method thereof The invention belongs to the field of medicinal preparations and particularly relates to a trimetazidine dihydrochloride sustained release tablet and a preparation method thereof. The trimetazidine dihydrochloride sustained release tablet takes polyvinyl acetate and mixture of povidone mixture and ethyl cellulose as sustained-release matrix materials and also contains a filling agent, a lubricating agent and other accessories. The release degree of the trimetazidine dihydrochloride sustained release tablet is not influenced by the granularity of raw material; the mixed sustained-release matrix material can be used for controlling the initial burst release of the trimetazidine dihydrochloride at earlier stage; the in vitro release of the sustained release tablet is not influenced by a pH environment; and meanwhile, the administration times of the medicament is reduced to two times from three times of general tablets, so that the administration adaptability of patients is improved. According to the preparation method of the trimetazidine dihydrochloride sustained release tablet, direct tabletting or granulation tabletting through a water-soluble solvent wet method can be adopted; and the preparation process is simple, and thus the trimetazidine dihydrochloride sustained release tablet can be continuously and stably produced in batch.
CN103402508A Dosages of arylsulfonamide derivatives The invention is directed to the therapeutic use of aryisuifonamide derivatives.
US20070275948 7-[4-(4-Chlorobenzyloxy)Benzenesulfonyl]-8-Methoxy-3-Methyl-2,3,4,5-Tetrahydro-1h-3-Benzazepinium Maleate Or Tosylate As antipyschotics The present invention relates to novel salts of 7-[4-(4-chlorobenzyloxy)benzenesulfonyl]-8-methoxy-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and a pharmaceutically acceptable solvate thereof, pharmaceutical formulations, processes for their preparation, and their use in medicine. The chemical entities are useful in therapy, in particular as antipsychotic agents.
US20100021552 Polysaccharide nanofibers having antimicrobial properties Polysaccharide nanofibers having anti-microbial properties, said nanofibers comprising an alginate and having silver nanoparticles dispersed throughout the nanofibers.
CN1989135A 3- (4- (2-dihydroisoxazol-3-ylpyridin-5-yl) phenyl) -5-triazol-1-ylmethyloxazolidin-2-one derivaives as mao inhibitors for the treatment of bacterial infections Compounds of formula (I) as well as pharmaceutically-acceptable salts and pro-drugs thereof are disclosed wherein R<1>, R<2>, R<3>, and R<4> are defined herein. Also disclosed are processes for making compounds of formula (I) as well as methods of using compounds of formula (I) for treating bacterial infections.
EP2661438A2 New bicyclic compound for modulating g protein-coupled receptors The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.
EP1681354A2 Recombinant viruses coding for a glutamate decarboxylase (gad) Recombinant defective virus contg. a DNA sequence (I) encoding a protein (II) with glutamate decarboxylase (GAD) activity, is new. Also new are:(1) a virus as above where the DNA is cDNA or gDNA which is under the control of a LTR-RSV promoter (which can be expressed in the majority of nerve cells);(2) a pharmaceutical compsn. contg. the virus;(3) mammalian cells infected with this virus, and(4) implants contg. these cells and an extracellular matrix.
US7691874 Treating symptoms of Parkinson's disease comprising administering an effective anti-Parkinsonism amount of 3-hydroxymorphinan (Norlevophanol); neuroprotectantsside effect reduction; cognition activators; Alzheimer's disease; drug abusepsychological disorders The present application discloses a pharmaceutical composition for treating Parkinson's disease and psychotropic intoxication/abusive potential, which contains a morphinan compound.
CA2179377C Method of treatment of hormone-unresponsive metastatic prostate cancer Prostate cancer particularly hormone-unresponsive metastatic prostate cancer, is treated by cyclophosphamide or other normally substantially inactive agent. Potentiation of the anti-cancer activity and amelioration of cyclophosphamide-associated toxicity is achieved by an initial intravenous infusion of DPPE over an approximately one hour period prior to cyclophosphamide treatment.
US7090874 comprises curcumin for preventing and/or improving Insulin Resistance Syndrome, diabetes mellitus, obesity or visceral fat obesity, hypertension or arterosclerotic cardiovascular disorders The object of the present invention is to provide PPARγ ligand derived from naturally occurring sources and a composition for preventing and/or improving Insulin Resistance Syndrome, diabetes mellitus, obesity or visceral fat obesity comprising the PPARγ ligand as an active agent. The present invention relates to a ligand for peroxisome proliferator-activated receptor which comprises curcumin or its derivatives. The composition according to the present invention, which comprises the PPARγ ligand as an active agent is useful for preventing and/or improving Insulin Resistance Syndrome, diabetes mellitus, obesity or visceral fat obesity.
WO2010127754A1 3-([1,2,3]triazole-4-yl)-pyrrolo[2,3-b]pyridine derivates The invention relates to compounds of the formula I, where R1, R2, and R3 have the meanings indicated in claim 1, wherein said compounds are inhibitors of PDK1 and cell proliferation/cell vitality, and can be used for treating tumors.
US20090022746 Complexes for transferring nucleic acids into cells The invention relates to complexes of cationic polymers and nucleic acids, to the use of such complexes for introducing nucleic acids into cells and organisms, to the use of the complexes as pharmaceuticals, and to novel polymers which can be used to prepare the complexes.
CN101605769A Thiazole compound (as ppard) ligand and pharmaceutical, cosmetic and health food comprised thereof The present invention relates to a thiazole compound as a peroxisome proliferator activated receptor d (PPARd) activator or pharmaceutically acceptable salts thereof, and a pharmaceutical composition, a functional cosmetic composition, a health food, health beverages, a food additive and animal feeds containing the same.
EP2468730A1 Substituted hydrazide compounds and application thereof The invention relates to substituted hydrazide compounds as shown by general formula I, including geometrical isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, and use of the same, wherein the substitutents Ar and R having the same meanings as given in the Description. T The invention further relates to the use of compounds of general formula I in the preparation of medicament for the treatment and/or prevention of cancer and other proliferative diseases.
CN1823804A Clamycin fast release micropill and its preparation method A quick-releasing micropill of clarithromycin contains clarithromycin, disintegrant, surfactant, adhesive, solvent, excipient and other medicinal additives.
WO2009131245A1 Iminopyridine derivatives and use thereof The present invention aims to provide an iminopyridine derivative compound having an α1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like.The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
CA2392877C Improvements in or relating to immune responses to hiv Disclosed is an immunogen in sterile form suitable for administration to a human subject, the immunogen comprising: at least a portion of the gag protein of HIV, said gag protein being from an HIV clade or having a consensus sequence for one or more HIV clades, and comprising at least parts of p17 and p24; and a synthetic polypeptide comprising a plurality of amino acid sequences, each sequence comprising a human CTL epitope of an HIV protein, and wherein a plurality of HIV proteins are represented in the synthetic polypeptide, said CTL epitopes being selected to stimulate an immune response to one or more HIV clades of interest.
EP1248774B1 Polyhydroxystilbenes and stilbene oxides as antipsoriatic agents and protein kinase inhibitors Disclosed herein are compositions containing hydroxylstilbenes or their derivatives or analogues. The compositions are useful to inhibit protein kinease, and for the treatment of inflammatory diseases, including psoriasis , multiple sclerosis, rhumatoid arthritis, restinosis, inflammatory bowel disease, and inflammatory lung disease. They are also useful to treat surgical adhesions and graft rejection. Novel derivatives and analogues are also disclosed.
US20120328540 Cysteinyl compounds, compositions and methods of use Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, the compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g., Parkinson's disease).
US20110082120 Substituted thioacetic acid salicylate derivatives and their uses The invention relates to substituted thioacetic acid salicylate derivatives; compositions comprising an effective amount of a substituted thioacetic acid salicylate derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a substituted thioacetic acid salicylate derivative.
CN1561988A Method for preparing taxol micro ball anti-cancer medicine An anticancer medicine in the form of microball is prepared through proportionally mixing taxusol and slow-releasing polymer in dark condition, stirring, ultrasonic dispersing, slowly dripping it in the aqueous solution of polyglycol, stirring, filtering to collect microballs, washing with distilled water, and drying. It can be mixed with the water for injection.
US7772241 fused pyrido[3'.2':4.5]pyrrolo[1.2-c]pyrimidine's used for treating cancer in mammals Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, NHSO2R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.
CN1951496A Use of long-acting human recombined soluble TNF alpha receptor in preparation of medicament for treating liver failure The invention relates to a method for preparing recombine soluble cancer necrotic factor alpha acceptor (Hus TNFR) gene drug. Wherein, the invention uses I or II type long-effect recombine soluble cancer necrotic factor alpha acceptor, via acute, sub acute liver exhaustion animal mode, to predict the liver exhaustion of mouse, and the result proves that it can prolong 10 times of semi-exhaustion period, with better treatment effect, then non-long-effect HusTNFR.
CA2585840A1 Use of an mtor inhibitor in treatment of uterine leiomyoma The invention provides for the use of an mTOR inhibitor in the treatment or inhibition of fibroids.
US8454984 Antimicrobial resin compositions Methods for making antimicrobial resins and for forming coatings comprising antimicrobial resins on substrate surfaces are disclosed. The methods involve providing a mixture comprising about 15 weight % to about 80 weight % of a hydrophilic acrylic oligomer, about 10 weight % to about 80 weight % of a multifunctional acrylic monomer, about 5 weight % to about 40 weight % of an adhesion-promoting acrylic or vinyl monomer, and about 0.1 weight % to about 15 weight % of a metal salt; and exposing the mixture to a radiation source to cure at least a portion of the mixture, thereby forming an antimicrobial resin.
WO2006002121A2 Compounds and methods for treating seizure and paroxysmal disorders This invention provides methods for alleviating paroxysmal disorders in an animal, particularly epilepsy, pain, migraine, syncope, bipolar disorders, psychosis, anxiety, a stress-induced disorder, by modulating glycolysis in brain cells. The preferred compound is 2-deoxy-D-glucose.
CN102641274A New application of madecassic acid The invention relates to a new application of madecassic acid, derivatives, and isomers thereof, and particularly relates to an application of madecassic acid and derivatives thereof, or compositions of madecassic acid or its derivatives and its isomers in the preparation of medicaments for prevention and/or treatment of breast-related diseases, or breast health-care products. Studies confirm that both oral administration and external use of madecassic acid or derivatives thereof or compositions of madecassic acid or its derivatives and its isomers have significant inhibition effect on breast hyperplasia of experimental rats.
CN1875954A An oral administered medicine for treating depression-Jin Yu Kang The invention relates to an oral medicament for treating depression prepared from effective components of Hypericum perforatum and characterized in that, the total content of Hypericin and Pesudohypedcin is 0.15-48%, the content of birutan is 2.3-4%, the content of total flavones is 50-90%, the content of Hyperforin is 2-46%. The dosage types of the oral preparation include tablets, capsules, powders and oral liquids.
US8609852 Thiazolyl mGluR5 antagonists and methods for their use The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
US20050222170 In combination with organic nitrate or nitric oxide donors or inhibitors of cyclic GMP metabolism; erectile dysfunction or female sexual dysfunction The invention relates to novel chemical compounds of formula (I), which stimulate soluble guanylate cyclase, to the production and use thereof as medicament, particularly in the treatment of cardiovascular diseases and/or sexual dysfunction (I), wherein R1″ represents chlorine, cyano, trifluoromethyl or methoxy and R2 represents hydrogen or fluorine or R1 represents fluorine and R2 represents fluorine. The invention also relates to the salts, isomers and hydrates of said compounds.
WO2009144394A8 Polysubstituted 2-aryl-6-phenyl-imidazo[1,2-α]pyridine derivatives, and preparation and therapeutic use thereof Compounds of Formula (I) (I), wherein: R1 is: a phenyl group or a naphthyl group, both groups capable of being optionally substituted; X is 1 to 4 substituents, identical to or different from each other and selected from hydrogen, halogen, (C1-C10)alkyl, halo(C1-C10)alkyl, (C1-C10)alcoxy, NRaRb, cyano, or nitro; R, in positions 3, 5, 7, or 8 of imidazo[1,2-a]pyridine, is 1 to 4 substituents, identical to or different from each other; R2 and R3, independently of each other, represent a hydrogen atom or an optionally substituted (C1-C10)alkyl group; an optionally substituted aryl group; R2 and X may form, together with the carbon atoms carrying them, a carbon ring of 5 to 7 carbon atoms; and R4 is a hydrogen atom, an optionally substituted (C1-C10)alkyl group, or an aryl group optionally substituted by one or a plurality of substituents. The invention is used in therapy and in methods of synthesis.
CN101138558B Pentamidine and death domain receptor ligand united application The present invention belongs to the pharmaceutical field. The present invention particularly relates to the medicine of pentamidine combined with the legend of the death structure receptor in treating the tumor and the leukemia. The ligand of the death structure receptor in the present invention comprises TRAIL, TNF-alpha or the analogues, which is the combination of the pentamidine with the metabolite or the analogues. The benefit of the present invention is that the pentamidine sensibility of the leukemia cell of the ligand of the death structure receptor. In the clinical field, when thepentamidine of the therapeutic drug concentration is applied in the leukemia cell, which is tolerant to the ligand of the death structure receptor, the apoptosis can be induced; therefore the purposefor the leukemia treatment is realized.
CN101991572B Novel dipeptidyl peptidase IV inhibitor The invention relates to a novel dipeptidyl peptidase IV inhibitor, which is N'-[(2-hydroxy-1-naphthyl)methylene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide, and has the structural formula shown in the description. The invention also provides a screening method and use of the novel dipeptidyl peptidase IV inhibitor. The novel dipeptidyl peptidase IV inhibitor has a novel structure and can effectively inhibit dipeptidyl peptidase IV, so the novel dipeptidyl peptidase IV inhibitor can serve as a medicine lead compound, and is used for preparing medicines for treating diabetes to benefit diabetics.
EP2258370A1 Treatment of malignant diseases The invention discloses the use of a 1H-indol-3-yl-compound with the formula (I) and any of its stereoisomeric forms or a mixture thereof wherein R1, R3, R4 and R5 are H; R7 is H or OH; A is CH2-CH2; B is 6-CH3-pyrimidine; R6 is H; and R7 is CHR8 (CH2) 3NR9R10; wherein R3 is CH3; R9 and R10 are C2H5; or a salt or solvate of a compound of formula (I) for the treatment of malignant diseases.
CN103622945A Use of garlicin in preparation of hyperlipoidemia treatment medicines The invention belongs to the field of medicines, and relates to a use of an enteric-coated garlic tablet in the preparation of hyperlipoidemia treatment medicines. The weight of the enteric-coated garlic tablet is 500mg, and the enteric-coated garlic tablet comprises 70wt% of lyophiled garlic powder and 30wt% of a pharmaceutical adjuvant, wherein the content of alliin in the lyophiled garlic powder is not lower than 30mg/g, and the pharmaceutical adjuvant contains a coating material. A high performance liquid chromatography result of the enteric-coated garlic tablet shows that the content of alliin in each tablet of the enteric-coated garlic tablet is 10-11mg, and the content of latent allicin in each tablet of the enteric-coated garlic tablet is greater than 5mg. The enteric-coated garlic tablet has the advantages of clear source, wide source, low price, easy obtaining, convenient administration, almost no pharmacological side effects, high bioavailability, safety and effectiveness; and the enteric-coated garlic tablet can avoid the irritation of high-content allicin to the upper gastrointestinal tract, and the garlic flavor does not escape from the oral cavity.
US20120309710 Compound sea cucumber preparation and manufacturing method thereof A sea cucumber preparation and manufacturing method thereof, comprising steps as follows: put the cut and well-cleaned fresh sea cucumber or soaked sea cucumber into an airtight container; at 70˜130° C., gelatinate for 1 min˜20 h, freeze-dry till the water content is less than 10 wt %, then sequentially carry out coarse, ultra-micro and nanometer crushing till the fineness reaches 10˜1000 nm. Add water into the sea cucumber nanometer powder to carry out proteinase enzymolysis, after the enzymolysis is finished, inactivate the proteinase, separate and take the supernatant and dry to get nanometer sea cucumber extract. Evenly mix the extract with panax pseudo-ginseng saponins extract at the proportion of 99˜70%:1˜30%. The content of the sea cucumber polysaccharide in the mixture is 2.5˜8.0 wt %, the content of panax pseudo-ginseng saponins is 0.3˜21.0 wt %. The compound preparation has complementary and synergistic effects on pharmacological effect. The side effects of single preparation can be eliminated through the compound preparation, the pharmacological functions of the sea cucumber or panax pseudo-ginseng single preparation are greatly enhanced, and can be used for anti-coagulation, diabetes and other various medicinal purposes.
CN102875504A Application of 4,5,6,7-tetrahydro pravastatin and salts thereof in cardiovascular diseases The invention relates to an application of 4,5,6,7-tetrahydro pravastatin and salts thereof in cardiovascular diseases, relates to the application of 4,5,6,7-tetrahydro pravastatin and the pharmaceutically acceptable salts thereof in preparing drugs, and particularly relates to the application of preparing drugs for treating hyperlipidemia. The 4,5,6,7-tetrahydro pravastatin and the pharmaceutically acceptable salts thereof have definite action targets and high hypolipidemic activity, and have no side effects of rhabdomyolysis of other statin-related drugs.
CN101837071A Composition of plant extracts and application in preventing or treating scars The invention relates to a composition of plant extracts for preventing or treating scars and application in preventing or treating skin scars. The composition comprises the following active ingredients in percentage by weight: 30 to 95 percent of asiaticoside, 4 to 35 percent of licorice root extract and 1 to 35 percent of green tea extract, wherein the composition accounts for 0.5 to 30 percent when applied to preparing external products of skin, and the composition is uniformly mixed with medically-acceptable excipients or carriers in proportion to prepare products in forms of gel, cream, serosity, aqueous solution agents, emulsions or solids. The composition has strong effect of preventing and treating the scars and small dosage under the combined action of the three active ingredients, and can avoid possible phenomena of pruritus and pain in the process of the healing of wound surfaces and reduce allergy rates and inflammation probability greatly, so that the color and luster of the skin at the healing position is more natural. The composition of the plant extracts can be added into medicaments or cosmetics for preventing or treating the scars by a known method used by technical personnel in the field, and is convenient to use.
US20100029595 Method of treating or preventing osteoporosis comprising administering to a patient in need thereof an effective amount of pharmaceutical composition comprising benzamidine derivatives or their salts, and alendronic acid or its salt The present invention relates to a pharmaceutical composition for preventing and treating osteoporosis, comprising N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}benzamidine, or salts thereof, and alendronic acid or a salt thereof. As a prophylactic or therapeutic composition for osteoporosis, the combination treatment of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, or salts thereof and alendronic acid or a salt thereof exhibits excellent inhibitory effect on osteoclast differentiation, as compared to each individual treatment, thereby being useful for the prevention or treatment of osteoporosis.
WO2013134348A1 Controlled-release solid dosage forms of mesalamine Described are controlled-release solid dosage forms of mesalamine. In one aspect of the invention the controlled-release solid dosage forms of mesalamine are capsules comprising a plurality of coated mini-tablets. Another aspect of the invention relates to a method of treating a patient suffering from inflammatory bowel disease, comprising the step of administering to the patient a therapeutically effective amount of the solid dosage form. The invention also relates to methods of inducing remission of inflammatory bowel disease and maintaining remission of inflammatory bowel disease. In certain aspects, the inflammatory bowel disease is ulcerative colitis or Crohn's disease.
US7297706 Certain glycine derivatives as factor Xa inhibitors for use in the treatment of thrombotic disorders Compounds of formula (I) in which R, R1, R2, n and X1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
WO2009105234A3 Methods and compositions for the treatment of disorders associated with defects of the cystic fibrosis transmembrane conductance regulator gene or protein The present invention features compositions, methods, and kits for treating, or ameliorating disorders associated with a defect in the cystic fibrosis transmembrane conductance regulator (CFTR) gene or protein (e.g., cystic fibrosis).
CN102228467A Application of hydrogen physiological saline in preparation for medicine treating acute neurological damage diseases The invention relates to an application of hydrogen physiological saline in the preparation for a medicine treating acute cauda equine damage diseases. The invention further provides an application of a hydrogen-contained oral liquid in the preparation for a healthcare product treating acute cauda equine damage diseases. The advantages of the application of the invention are as follows: the new use of hydrogen physiological saline is developed, as well as an acute neurological damage protection function similar to that of methylprednisolone and a treatment effect to acute cauda equina syndrome of the hydrogen physiological saline are found; the hydrogen physiological saline is featured with simple preparation, high injection concentration, convenient use, no explosion risk, very low cost, no side effect and good treatment advantage, which greatly reduces the medicine side effect risk of the acute neurological damage patient and greatly decreases medical costs; the invention further develops a new use of the hydrogen-contained oral liquid, wherein the hydrogen-contained oral liquid is simply prepared, convenient for the patient to drink and with no toxic and side effects as well as great advantage to treat the acute cauda equina syndrome.
WO2005087749A1 2-aminoquinazoline derivative A 2-aminoquinozoline derivative represented by the formula (I) (wherein R1 and R2 are the same or different and each represents hydrogen, (un)substituted lower alkyl, etc.; R3 represents (un)substituted aryl, (un)substituted aromatic heterocyclic group, etc.; R4 and R5 are the same or different and each represents hydrogen, halogeno, (un)substituted lower alkyl, (un)substituted aryl, etc., provided that not both are hydrogen; and R6represents hydroxy or (un)substituted lower alkoxy) or a pharmacologically acceptable salt of the derivative.
CN102656148A Cyclic hydroxylamine derivatives, their preparation and use as antioxidants The present invention concerns cyclic hidroxylamine derivatives of formula (I), and the salts thereof. Said derivatives have proved to be particularly effective as antioxidants for treating cellular oxidative stress, particularly in the brain.
CN101600440A Pharmaceutical composition comprising a pyrazole-O-glucoside derivative The invention relates to a pharmaceutical composition comprising a pyrazole-O-glucoside derivative selected from the group of compounds (1) to (29) according to claim 1 in combination with at least one second therapeutic agent which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
CA2749700A1 Benzodiazepin-2-on derivatives The present invention relates to a compound represented by the formula(I): wherein R1 represents a hydrogen atom or the like;R2 represents lower alkyl or the like;R3 and R4 represent lower alkyl or the like;R5 represents phenyl or the like;R6 rep-resents a hydrogen atom or the like;m is an integer of from 0 to 2;p is an integer of from 1 to 4; and q is an integer of from 1 to 5, or a pharmaceutical acceptable saltthereof, and a DGAT 1 inhibitor comprising the compound.
EP2000136A2 Compositions and methods for the treatment of inflammatory diseases using topoisomerase inhibitors Topoisomerase inhibitors are useful for the treatment of inflammatory disorders including arthritis, restonosis, surgical adhesions and other diseases. Controlled release polymeric formulations to topoisomerase inhibitors are particularly suitable for this use.
US7696186 7,9-substituted tetracycline compounds The present invention pertains to novel 7,9-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
CN101569631A Anti tumor application of 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound The invention relates to an application of 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound for inhibiting gastric cancer cell SGC-7901 and hepatoma cell BEL-7404. Experiments show that 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound can inhibit the proliferation of gastric cancer cell SGC-7901 and hepatoma cell BEL-7404 with an obvious effect and can be used to prepare antineoplastics. Electrophoresis detection shows that by increasing the expression quantity of apoptosis-related gene Bax, the 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound can improve the apoptosis of hepatoma cell BEL-7404.
US20110077572 Medical Equipment and Products using Chlorine, Hydrogen Peroxide, and Anti-Viral, Anti-Bacterial, Anti-Fungal, Agents, usage Method Improvements Dread Disease Cures, Remissions, and Anti-Infective Treatment Measures, Disease Treatment and Prevention System Chlorine and Hydrogen Peroxide Medical Therapies including Ear Dropper Multiple Vile Medicine Mixing Cool Mist Vaporizer with detachable Inhalation Hose and Facemask Double Density Air Filter, 3-Speed Motor with On/Off Switch, Home and Hospital Models with Atomizer and an Orifice for attachment to and Oxygen Tank, Pre-Wrapped Bandages, Gauze Stick-On Strips or Squares or Strip-less Gauze Pads with Liquid or Gel, Chlorine or Hydrogen Peroxide also, Lotions for Skin Infections and Cancers, Chemical Injections and Patient Baths, and Wellness Therapies
CN103181947A 4-component botanical medicine composition for treating liver fibrosis, and preparation method thereof The invention relates to a 4-component botanical medicine composition for treating liver fibrosis, and a preparation method thereof. The 4-component botanical medicine composition comprises the following components by weight per kg: 180-350 mg of crude cordyceps polysaccharide, 0.06-0.82 ml of cordyceps liposoluble components, 2-68 mg of gypenosides and 3-12 mg of gynostemma pentaphyllum polysaccharide. The preparation method comprises the following steps: step 1, extracting the crude cordyceps polysaccharide, the cordyceps liposoluble components, the gypenosides and the gynostemma pentaphyllum polysaccharide respectively; and step 2, preparing a botanical medicine primary liquid and various clinical preparations according to the compatible dosage. The 4-component botanical medicine composition can obviously improve the curative effect, reduce the side effect and has a good clinical application prospect.
CA2295628C Stable formulations comprising a nucleotide and a freeze drying additive A pharmaceutical composition comprising a nucleotide analogue and one or more glass forming additives which is suitable for freeze drying.
EP2268641A2 Heterocyclic compounds as adenosine receptor antagonist Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.
US20100216833 Tetrahydrocarbazoles and derivatives The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXRα and/or LXRβ agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.
CN101564386A Novel applications of pinane amine as M2 inhibitor in pharmacy The invention discloses applications of pinane amine with a formula I or receivable salt of the pinane amine in pharmacy which are taken as an M2 inhibitor in the preparation of drugs for preventing and curing influenza and a compound containing the pinane amine with the formula I or the receivable salt of the pinane amine in pharmacy. The pinane amine or the receivable salt or the compound of the pinane amine which is taken as an M2 ion channel protein inhibitor can block the virus reproduction and is used for curing the influenza, in particular to influenza A.
CA2670964A1 Use of composition for manufacture of medicant and method for inhibiting formation of body fat The present invention relates to use of a composition for the manufacture of a medicament and a method for inhibiting the formation of body fat. The composition includes lactoferrin and a trivalent chromium compound. Herein, the chromium compound is selected from the group consisting of chromium (III) chloride hexahydrate, chromium (III) chloride, chromium (III) acetate, chromium (III) sulfate, chromium picolinate, chromium nicotinate, chromium GTF, chromium yeast extract, other inorganic salts of trivalent chromium, other organic salts of trivalent chromium, and combinations thereof. Accordingly, the composition of the present invention can assist in transmitting glucose from cells to muscle tissues and thereby reducing the storage of fat converted from glucose to achieve the purpose of controlling body weight.
WO2014128093A1 Substituted-imidazo[1,2-b]pyridazines as mknk1 inhibitors The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): (Ia) (Ib) (Ic) (Id) in which A, Y, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
EP2065053A1 Cell death inhibitor The present invention relates to an antioxidant response element (ARE) activator comprising a macrophage migration inhibitory factor (MIF) or a modified form thereof, an ARE activator comprising a combination of MIF or a modified form thereof and a substance capable of binding to MIF, and so on. These ARE activators are useful as safe and excellent cell death inhibitors, such as agents for the prevention/treatment of cardiovascular diseases, bone/joint diseases, infectious diseases, inflammatory diseases, renal diseases, central nervous system diseases, cancer or diabetes.
WO2013147232A1 Bionanocapsule having antibody against surface protein of dendritic cell The purpose of the present invention is to provide a vaccine which can meet a market need satisfactorily. The purpose can be achieved using a bionanocapsule which has an antibody against a surface protein of a dendritic cell and also has a virus-like particle containing a virus surface antigen protein.
CN1618869A Polysaccharide of basidium and its use A polyose of antrodia cinnamonea basidiomycetes is prepared from the strains CCRC 35396, CCRC 35398, B71, B85 and B86 of antrodia cinnamonea, and can be used to prevent the treat viral hepatitis B.
WO2010111108A3 Compositions and methods for the treatment of wounds The present invention is directed to a wound composition comprising an effective amount of phenytoin and an effective amount of vitamin C. The present invention is further directed to a method of treating a wound in a patient comprising administering an effective amount of phenytoin and an effective amount of vitamin C to the wound.
US7169774 Purification of natural, synthetic or semi-synthetic crude harringtonines by reverse phase chromatography and crystallization; solvent is water or lower alkanol, or an aqueous mixture of organic solvents; enantiomerically pure; industrial scale; leukemia chemotherapy The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and functionalization are entirely preformed. The invention also concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n=2 (i.e. harringtonine) or n=3 (i.e. homoharringtonine), in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97.5%.
WO2008124524A3 Aryl sulfonamide compounds as modulators of the cck2 receptor Certain aryl sulfonamide compounds are CCK2 receptor modulators useful in the treatment of CCK2 receptor-mediated diseases.
WO2010026134A1 Triazole derivatives and their use as nicotinic acetylcholine receptor modulators This invention relates to novel triazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
WO2012176878A1 Proteasome inhibitor [Problem] To provide a novel proteasome inhibitor which can be administered orally. [Solution] A proteasome inhibitor comprising, as an active ingredient, a compound represented by general formula (1) [wherein Y and Y' are the same as or different from each other and independently represent a single bond, -O-, -NH-, -CH=CH→, -CO-CH=CH→, -O-CONH→, -S-CO→, -CONH→, -NHCO→ or NHSO2→ [wherein "→" represents a bond located on the phenyl group side]; R1, R2, R3, R4, R5, R6, R7 and R8 are the same as or different from one another and independently represent a hydrogen atom, a halogen atom, a hydroxy group, an amino group, a carboxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkoxycarbonyl group; R9 and R10 are the same as or different from each other and independently represent a hydrogen atom or a C1-6 alkyl group, or R9 and R10 together form -CH2CH2- or -CH2CH(R11)CH2- [wherein R11 represents a hydrogen atom, a C1-6 alkoxy group or a C1-6 alkylsulfonyloxy group]; and m and n are the same as or different from each other and independently represent an integer of 2-4] or a salt thereof, or a solvate of the compound or the salt.
CN1919179A Anticancer slow release preparation of nimustine and its progression agent Disclosed is slow release anticancer agent carrying both Nimustine and its synergistic agents, which comprises slow release auxiliary materials and active anticancer constituents, wherein the active anticancer constituents include Nimustine and its synergistic agents (such as Vinblastine, Goserelin or Carmofur). The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved. The solid tumors include glioma, osteosarcoma, lymphoma, lung carcinoma, intestinal cancer, and breast cancer.
US20080070975 methylnaltrexone, a calcium salt, chelating agent in aqueous solution; calcium salts of EDTA, DTPA, HEDTA, EGTA, nitrilotriacetic acid or calcium citrate; reducing severity of side effects from use of analgesic opioids; effective delivery without degradation under refrigeration and/or room temperature The present invention provides formulations that achieve effective delivery of methylnaltrexone compositions. The provided formulations are useful for preventing, treating delaying, diminishing or reducing the severity of side effects resulting from use of analgesic opioids.
US8574634 Compositions and methods of treatment with proanthocyanidin polymer antidiarrheal compositions Pharmaceutical compositions containing a proanthocyanidin polymer composition which are useful for the treatment and prevention of secretory diarrhea are provided. The invention specifically relates to pharmaceutical formulations of a proanthocyanidin polymer composition which has been isolated from a Croton spp. or a Calophyllum spp. In particular, the invention relates to a formulation of a proanthocyanidin polymer composition which protects the composition from the effects of stomach acid after oral administration, particularly to those formulations which are enteric coated. The invention also relates to methods of producing a directly compressible proanthocyanidin polymer composition, as well as compositions containing the directly compressible proanthocyanidin polymer composition.
CA2116388C Treatment for viral diseases An angiotensin II antagonist compound is administered to mammals with viral disease. This administration ameliorates virus-associated cell injuries, producing therapeutic effects in viral diseases. This compound is also useful for the prevention of such diseases. The angiotensin II antagonist compound is, for instance, of the formula: (see formula I) or a pharmacologically acceptable salt thereof, wherein the ring is a benzimidazole ring which may be substituted, R3 is a group capable of forming or transformable to an anion, X is a bond or a spacer of a chain having up to 2 atoms and n is 1 or 2.
WO2012080329A1 Formulations of n-(3,5-dichloropyridin-4-yl)-[1-(4-fluorobenzyl)-7-azaindol-3-yl)]glyoxylic acid amide The present invention relates to a pharmaceutical composition comprising (i) N-(3,5-dichloropyridin-4-yl)-[1-(4-fluorobenzyl)-7-azaindol-3-yl)]glyoxylic acid amide (ELB353, Ronomilast), (ii) a binder material and (iii) a carrier material. The invention also relates to a process for preparing the composition. Further, the invention relates to the composition for use particularly in the treatment and/or prophylaxis of chronic obstructive pulmonary disease (COPD).
EP2536398A1 Treatment of osteoporosis According to the invention there is provided a compound of formula (I): wherein R1, R2, R3 and n have meanings given in the description, or a pharmaceutically acceptable solvate, salt or prodrug thereof for use in the treatment of osteoporosis and/or osteopenia.
CN1985958A Slow released capsule of netilmicin sulfate and bletilla tuber glue for animal and birds The present invention belongs to the field of veterinary medicine technology, and is especially slow released veterinary medicine capsule prepared with netilmicin sulfate and bletilla tuber as material. The preparation process includes the following steps: water extracting and alcohol precipitating to extract bletilla tuber glue; mixing netilmicin sulfate and bletilla tuber in the ratio of 1 to 3 and 10 % concentration alcohol solution of PVP as adhesive; making pellet of 20 meshes and encapsulating. The slow released veterinary medicine capsule has long medicine retaining time in the disease focus, high local medicine concentration, excellent bioadhesion and obvious medicine slow releasing characteristic.
WO2012125623A2 Cleavage inhibitors of transforming growth factor beta type i receptor and uses thereof in cancer therapy Disclosed herein are methods to inhibit cleavage of a type I receptor of transforming growth factor beta (ΤβRI) and reduce cancer cell invasiveness/metastasis, and agents and pharmaceutical compositions for use in these methods. Also disclosed herein are methods for identifying agents that inhibit cleavage of ΤβRI and methods for diagnosing and/or prognosing cancer based on nuclear localization of a intracellular domain of ΤβRI, which is a product of ΤβRI cleavage.
US8052984 Increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of the skin and skin appendages The invention is an increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages. The allylamine active ingredient is prepared in an acidic environment; the acidic environment altering the physiochemical properties of the active ingredient resulting in the active ingredient having a positive charge. The positive charge and enhancers used in the formula allow for increased penetration of the active ingredient through skin and skin appendages. The positively charged active ingredients are either dissolved in the vehicle directly or dissolved in a plurality of beads suspended in the vehicle. The bead structure minimizes the molecular diffusion of the positively charged active ingredient and a catalytic species through the bead structure, thus stabilizes the positively charged active ingredient inside the bead by impeding the interaction of the positively charged active ingredient and the catalytic species, and thereby extending the shelf life of the positively charged active ingredient.
CA2773579A1 Medicament including antibody composition specifically bound to human cc chemokine receptor 4 (ccr4) There is a demand for a medicament which includes a genetically recombinant antibody specifically bound to human CC chemokine receptor 4 (referred to as CCR4 hereinafter) and at least one type of medicinal agent, and also for a medicament for administering a genetically recombinant antibody for CCR4 combined with at least one type of medicinal agent. Provided are a medicament which includes a genetically recombinant antibody specifically bound to CCR4 and at least one type of medicinal agent, and a medicament for administering a genetically recombinant antibody for CCR4 combined with at least one type of medicinal agent.
US20110190281 Sulfone substituted 2,3-dihydroimidazo [1,2-c] quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis This invention relates to novel sulfone 2I3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis mediated disorders, as a sole agent or in combination with other active ingredients.
CN102240264A Application of poly(cinnamic alcohol) injection used as cyst treatment medicament The invention belongs to the technical field of poly(cinnamic alcohol) injection medicament application, and in particular relates to application of a poly(cinnamic alcohol) injection used as a cyst treatment medicament. Conventional cyst treatment methods mainly comprise surgical excision, laparoscopic excision and others, with the disadvantages of long incision, multiple bleeding, severe wound, high cost and easy recurrence. In the application of the poly(cinnamic alcohol) injection used as the cyst treatment medicament provided by the invention, the medicament therapy is used to replace surgery therapy, 1% of the poly(cinnamic alcohol) injection is injected into the endothelial cells with the secretory function in the cyst wall, thus resulting in aseptic inflammation and the cyst is solidified, hardened, adhered, closed and gradually absorbed so as to disappear. According to the invention, the cyst patients can be treated without hospitalization, and the high cyst recurrence rate caused by incomplete surgical excision is avoided.
US8501110 uniform heating and cooling of the containers, preventing stress cracks; gentle; use of radiant heat-generating heating units that act on the container bottoms in concert with the hot air from the ventilating fan units A sterilizing tunnel for pharmaceutical containers has an entry zone, a heating zone, and two cooling zones. The individual zones contain ventilating fan units that generate air currents, which serve to heat and cool the containers that a transport apparatus conveys through the sterilizing tunnel. The heating and cooling units, which operate using the principle of heated and cooled air flow, is supplemented with radiant heat-generating unit. The sterilizing tunnel makes it possible to achieve a uniform heating and cooling of the containers, preventing stress cracks in the containers and permitting intentional heating that makes it possible, for example, for the containers to be coated with a substance.
WO2012165995A1 Photodynamic treatment method for malignant tumors The invention relates to medicine and can be used in oncology for the treatment and prophylaxis of malignant tumors of the skin and mucosa, and also in ophthalmology for the treatment and prophylaxis of intraocular tumors. In order to increase the effectiveness of treatment and prophylaxis of malignant tumors by optimizing the process of delivering a preparation to the critical organ, in the photodynamic treatment method for malignant tumors according to the invention, which includes administration of a photosensitizer and photoirradiation of the tumor, performed after the aforesaid administration, at a wavelength corresponding to the maximum absorption of chlorine derivatives, a gelatin capsule filled with microparticles of a powder of chlorine derivatives mixed with lyophilized spirulina platensis is used as the photosensitizer, wherein each microparticle of powder is coated with a protective, acid-resistant film, and the gelatin capsule is administered orally. Furthermore, a Kollicoat-type coating is used as the protective, acid-resistant film, and a calcium stearate powder is used to prevent the microparticles from clumping. Each gelatin capsule contains components in the following proportions by weight (mg): 1-1.5 chlorine derivatives; 100-150 spirulina platensis; 50-75 protective acid-resistant film; 0.5-0.75 calcium stearate.
US6964780 Phosphodiesterase inhibitor; therapy for sexual disorders; sildenafil in polyoxyethylene glycol enteric coating The invention provides controlled-release formulations for oral administration containing a cGMP PDE-5 inhibitor. The formulations are useful, inter alia, in the treatment or prevention of sexual dysfunction.
WO2011089167A1 Kombination of proteasome inhibitors and anti -hepatitis medication for treating retroviral diseases The present invention relates to use of proteasome inhibitors in combination therapy with further anti-retroviral compounds for treating retrovirus infections such as HIV-infections and diseases or conditions induced by a retroviral infection, e.g. AIDS.
WO2012041959A1 Treatment of b-cell lymphoma with microrna The invention relates to microRNA-34a and related microRNAs for use in the treatment of B-cell lymphoma. Likewise it relates to microRNA-34a for use in the preparation of a medicament for the treatment of B-cell lymphoma, and for a method of treatment of B-cell lymphoma comprising administering microRNA-34a. These claims are based on the observation that microRNA-34a shows strong anti-proliferative effects when overexpressed in diffuse large B-cell lymphoma (gDLBCL) cell lines, or when delivered intratumorally or systemically in xenograft models of DLBCL.
EP2503993A1 4-[2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine salts The present invention relates to 4-[-2-[[5-methyl-1 -(2-naphthalenyl)-1 H-pyrazol-3- yl]oxy]ethyl]morpholine salts, specifically to the hydrochloride, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of sigma receptor associated diseases.
US20120029074 Controlling transgene expression across the skin The invention relates to the use of a skin permeating compound such as phloretin for controlling transgene expression under control of the Pseudomonas putida DOT-T1E-derived bacterial repressor TtgR, to a vector comprising the genetic code for the repressor TtgR fused to a transactivation or a transrepressor domain, to a vector comprising a TtgR-specific operator sequence (OTtgR), a promoter and a polynucleotide coding for an endogenous or exogenous protein, and to a mammalian cell transiently or constitutively transfected with the mentioned vectors, and to mammals comprising such cells in nano- or microcontainers.
US20070270446 Reversed Pyrimidinone Compounds as Calcilytics Calcilytic compounds and methods of preparing them are disclosed. Methods of using the calcilytic compounds are also provided.
US20120088753 Pyrrolopyrimidines and used as kinase inhibitors The invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is —NR7(CO)R11; R2 is aryl, heteroaryl, fused aryl-C3-6-heterocycloalkyl or fused heteroaryl-C3-6-heterocycloalkyl, each of which is optionally substituted; each R7 is selected from hydrogen, C1-6-alkyl and C3-7-cycloalkyl, wherein said C1-6-alkyl is optionally substituted by one or more halogens; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6alkyl-C3-7-cycloalkyl, Ĉ-heterocycloalkyl, aryl and heteroaryl, each of which may be optionally substituted. Further aspects of the invention relate to pharmaceutical compositions comprising the same, and methods for treating or preventing a disorder selected from cancer, septic shock, Primary open Angle Glaucoma (POAG), hyperplasia, rheumatoid arthritis, psoriasis, artherosclerosis, retinopathy, osteoarthritis, endometriosis, chronic inflammation and Alzheimer's disease. Another aspect of the invention relates to the use of a compound as described above in the preparation of a medicament for the prevention or treatment of a disorder caused by, associated with or accompanied by any abnormal kinase activity, wherein the kinase is selected from TBK1, ERK8, CDK2, MARK3, YES1, VEG-FR, IKKepsilon and combinations thereof.
US20100261683 Selective Inhibitors for Cyclin-Dependent Kinases This invention provides a class of compounds which are useful for specifically inhibiting cyclin-dependent kinases. This class of compounds finds use in treating diseases resulting from inappropriate activity of cyclin-dependent kinases, including cancer, viral infections (e.g., HIV) neurodegenerative disorders (e.g. Alzheimer's disease), and cardiovascular disorders (e.g. atherosclerosis). Moreover, certain members of this class are particularly useful for inhibiting cyclin-dependent kinase 7 and are especially useful for the treatment of breast cancer.
WO2014117741A1 Heterocyclo compounds as apoptotic inducers and uses thereof Disclosed are heterocyclo compounds that have a formula represented by the following: and wherein X, R1, R2, R3, R4, R5, R6, and n are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of cancer conditions in mammals including humans, including by way of non-limiting example, prostate, colon, bladder, melanoma, liver, breast, cervical, ovarian, esophagi, glialblastoma, pancreatic and lung cancer.
CN1575797A New use of medicine containing escin and its salt The present invention relates to the new pharmaceutical use of aescin andits salt, and is especially the application of aescin and its salt in preparing post-operation intestinal function recovering medicine. The medicine of aescin and its salt is administrated via intravenous injection.
US20080234278 Beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and their use as pharmaceutical compositions.
US20070099832 Combination Therapy with p38 MAP Kinase Inhibitors and their Pharmaceutical Compositions The present invention relates to pharmaceutical combinations therapies based on p38 kinase inhibitors and another active ingredient, pharmaceutical compositions comprising such combinations, processes for preparing them and their use in the treatment of cytokine mediated diseases.
WO2008001752A1 Treatment of chronic obstructive pulmonary disease by statin Disclosed is a pharmaceutical composition for treatment or prevention of chronic obstructive pulmonary diseases. The pharmaceutical composition contains an HMG-CoA reductase inhibitor as an active ingredient.
CN103751089A Secnidazole quick-release preparation The invention provides a secnidazole quick-release preparation, which contains 5-10 wt% of secnidazole and the balance of water-soluble carriers including PEG 4000, PEG 6000 and poloxamer 188. A preparation method of the quick-release preparation provided by the invention comprises the following steps: mixing polyethylene glycol 4000 and polyethylene glycol 6000, heating and melting to obtain a mixed matrix A; mixing and melting secnidazole and poloxamer 188 to obtain a drug-containing mixed matrix B; fully mixing the mixed matrix A with the drug-containing mixed matrix B; transferring the mixture to a liquid storage bottle; sealing and insulating at 80-90 DEG C; regulating a dropping liquid quantitative valve, dropwise adding the mixture into liquid paraffin of 10 DEG C-15 DEG C from the top down; draining the formed quick-release preparation, erasing the liquid paraffin; and drying in a lime cylinder to obtain the preparation.
US20120129831 Substituted 3-(1,2,4-Oxadiazol-5-yl)-5-Phenylpiperidines The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.
CN101366805A Medicament composition for preventing birth defect and improving memory and intelligence The invention relates to a medical composition for preventing birth defects and improving memory and intelligence, which comprises Langehead Atractylodes Rhizome, rhodiola, vitamin B complex, and trace elements of zinc and selenium. The medical composition is mainly suitable for pregestational women, pregnant women and wet nurses, is very effective in preventing the birth defects and improving the memory and the intelligence, has both health care and tonic efficacies, and does not generate any side effects even after long-term application.
US8715701 Microstructural protein preparations containing adsorbed biologically active substances and their application in medicine and cosmetics Protein preparations containing biologically active compounds and the application of the protein preparations obtained, particularly as a component of medicinal and cosmetic preparations as protective substances or in the regeneration of cells and tissues of the human organism, and which can comprise a component of culture media for dermal or hepatic tissues, or for stem cells destined for use in the regeneration of cells and tissues in the human organism.
US20050010050 Antiinflammatory agents; antiarthritic agents; anticancer agents; analgesics A class of dihydrobenzopyrans, dihydrobenzothiopyrans, tetrahydroquinolines, tetrahydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula (I) wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.
US20100179227 Production method of hop preparation, hop preparation, anti-inflammatory agent, food product and beverage, and oral product A method for producing a preparation that can be used in the prevention and treatment of inflammatory diseases, including periodontitis caused by P. gingivalis. Specifically, the invention provides a method for producing a hop preparation comprising the following steps (1) to (3): (1) adjusting the pH of a polyphenol-containing liquid prepared from hop bracts to 6 to 7 and passing the liquid through a gel-type synthetic resin to allow components including useful substances to be adsorbed onto the resin; (2) washing the resin obtained in the step (1) with a 30 to 60% aqueous ethanol solution to elute unwanted substances, leaving the useful substances adsorbed to the resin; and (3) washing the resin obtained in the step (2) with a 70% or higher aqueous ethanol solution or ethanol to elute the components including the useful substances and forming the preparation from the eluted fraction.
EP2205243A2 Mast cell stabilizers in the treatment of obesity The present invention is directed to methods of treating or preventing the development of obesity by administering compounds that stabilize mast cells, hi addition, it includes pharmaceutical compositions which have both a mast cell stabilizer and instructions regarding the use of the stabilizer in treating or preventing'obesity.
EP2351742A1 Indazole derivative Compounds represented by the Formula (A-1) and the Formula (1) or salt thereof are provided. The compounds represented by the Formula (A-1) and the Formula (1) or salt thereof have a β3 adrenergic receptor agonist activity, and therefore are useful as an agent for the prevention and treatment of diabetes, obesity, hyperlipidemia, depression, biliary stone, a disorder derived from hyperactivity of biliary tract, a disorder derived from hyperactivity of digestive tract, interstitial cystitis, overactive bladder, urinary incontinence or a disorder derived from decreased tear secretion, etc.
EP1097138B1 Pharmaceutical compositions comprising 2-quinolones The invention concerns a pharmaceutical composition having an activity on the proliferation of clonogenic cells in tumours and comprising an efficient amount of a compound selected among the compounds of formulae (I) and (Ia) wherein: X, R1, R2, R3, R4, R5, R6 are as defined in Claim 1.
US20100311704 Pharmaceutical delivery systems for treatment of substance abuse and other addictions Disclosed are injectable pharmaceutical compositions that contain a therapeutically effective amount of an anti-addictive agent, an anti-inflammatory agent, and a pharmaceutically acceptable liquid carrier, methods of making the compositions, and uses thereof for treating addictions including substance abuse (or addiction to an abused substance) and addictive or compulsive behavior, by administering the composition to a subject in need thereof.
CA2834610A1 Rna interference mediated inhibition of isocitrate dehydrogenase (idh1) gene expression The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of IDH1 and mutant IDH1 gene expression and/or activity, and/or modulate an IDH1 or mutant IDH1 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules, including small nucleic acid molecules such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules, that are capable of mediating or that mediate RNA interference (RNAi) against IDH1 or mutant IDH1 gene expression.
WO2008117801A1 Composition for cartilage protection [PROBLEMS] To provide a composition for cartilage protection which has a high safety and an improved cartilage protection effect. [MEANS FOR SOLVING PROBLEMS] A composition for cartilage protection characterized by comprising, as the active ingredient, water-soluble heteropolysaccharides produced by an acetic acid bacterium (for example, an acetic acid bacterium belonging to the genus Acetobacter), preferably water-soluble heteropolysaccharides AX-1 and/or water-soluble heteropolysaccharides AM-2 or decomposition products (for example, degradation products) of these polysaccharides. This composition is also usable as a food, a drink and/or a drug.
US20080069896 Side effect reduction; reduced toxicity; fine particle size; blend of platinum chloride or chloroplatinic acid with apatite Antitumor agents with high antitumor effect have much side-effect, and its activity decreases when the toxicity decreases. Thus, satisfactory antitumor effects are not always obtained. Therefore, development of an antitumor agent having a high antitumor effect, with less side-effect and low toxicity is awaited. The present invention is to provide an antitumor agent of fine particles, wherein platinum chloride, chloroplatinic acids and hydroxyapatite are blend. Platinum chloride and chloroplatinic acids are platinum tetrachloride, tetrachloroplatinate, hexachloroplatinate, disodium platinum tetrachloride, disodium platinum hexachloride, dipotassium platinum tetrachloride, or dipotassium platinum hexachloride. The maximum particle diameter of hydroxyapatite is 1 μm or less.
WO2009112678A3 Azabicyclic carboxamide derivatives, preparation thereof and therapeutic use thereof The invention relates to the compounds of general formula (I) in which X1, X2, X3 and X4 are, independently of one another, a nitrogen atom or a C‑R1 group; Z1, Z2, Z3 and Z4 are, independently of one another, a nitrogen atom or a C‑R2 group; Ra and Rb form, together with the carbon atoms which bear them, a five-membered ring, this ring comprising a nitrogen atom and carbon atoms, this ring being partially saturated or unsaturated and being optionally substituted with one or more substituents R3; W is an oxygen or sulphur atom; n is equal to 0, 1, 2 or 3; Y is an optionally substituted aryl or heteroaryl; in the form of a base or of an addition salt with an acid, and also in the form of a hydrate or of a solvate. Process for the preparation thereof and therapeutic use.
WO2009147211A1 New compounds v The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
CN101072762B Phenyl-piperazin methanone derivatives The present invention relates to compounds of the general formula (I) wherein R<1> is the group (A) or (B) or (C) or (D); R<2> is a non aromatic heterocycle, or is OR' or N(R'')2; R' is lower alkyl, lower alkyl substituted by halogen or -(CH2)n-cycloalkyl; R'' is lower alkyl; R<3> is NO2, CN or SO2R'; R<4 >is hydrogen, hydroxy, halogen, NO2, lower alkyl, lower alkyl, substituted by halogen, loweralkoxy, SO2R' or C(O)OR''; R<5>/R<6>/R<7> are hydrogen, halogen, lower alkyl or lower alkyl, substituted by halogen; X<1>/X<1'> are CH or N, with the proviso that X<1>/X<1'> are not simultaneously CH; X<2> is O, S, NH or N(lower alkyl); n is 0, l or 2; and to pharmaceutically active acid addition salts and to their use in the treatment of neurological and neuropsychiatric disorders.
EP0975608B1 Halo-alkoxycarbonyl prodrugs Halo-alkoxycarbonyl derivatives of formula (I) are provided as prodrug moieties for pharmaceutical agents containing a basic or polar nitrogen containing fucntionality. The prodrugs are provided as pharmaceutical compositions as well as in methods of treatment. A compound of said formula wherein [(H)0-2(X)1-3] is selected from the group consisting of X3, HX2, and H2X and X2 is a halogen selected from the group consisting of F, Cl, Br, I or a combination thereof; R?2 and R3¿ are the same or different and are selected from the group consisting of H, C¿1?-C4alkyl, C1-C4alkoxy, cyano, halo(F, Cl, Br, I) C1-C4alkyl and aryl, AG-Q is a biologically active pharmaceutical agent wherein Q is a basic N-containing functionality selected from the group consisting of an amino, amidino, aminoalkyleneamino, iminoalkyleneamino, and guanidino group.
WO2013045962A1 Pharmaceutical composition for the prevention and/or treatment of muscle atrophy The invention refers to the use of compound of formula I or an N-oxide of the compound of formula I or a pharmaceutically suitable acid addition salt thereof for the preparation of a pharmaceutical composition for the prevention and/or treatment of muscle atrophy.
US8487009 1,2-diphenylethene derivatives for treatment of immune diseases The invention provides novel 1,2-diphenylethene derivatives and pharmaceutically acceptable salts thereof, the process for production of these compounds and their pharmaceutical composition and the use of these compounds as modulators of T-cells, neutrophils, macrophages and their associated cytokines as agents for treating immune, inflammatory and auto-immune diseases.
US20110172289 Minor groove binder (mgb)-oligonucleotide mirna antagonists Compositions and methods for inhibiting the actions of non-coding RNAs such as miRNAs and piRNAs are provided. The compositions comprise single or double stranded oligonucleotides conjugated with Minor Groove Binders (“MGBs”). The oligonucleotides can vary in length, can contain nucleotides having one or more modifications, and have regions that are substantially complementary to one or more mature miRNAs or piRNAs.
US7319097 Treatment of type II diabetes with benzenesulfonamide substituted with an N-heterocycle: N-[2-amino-5-(1,4-diazepan-1-yl)phenyl]benzenesulfonamide, N-[4-amino-5-(piperazinyl)phenyl]benzenesulfonamide, 3-amino-4-(5-methyl-2,5-diaza-bicyclo[2.2.1]hept-2-yl)-N-phenyl-benzenesulfonamide hydrochloride The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system
US20080306057 P13K Inhibitors for the Treatment of Endometriosis This invention relates to a method of treating and/or preventing endometriosis comprising administering a PI3K inhibitor. The PI3K inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis-related infertility.
USRE41339 N-acetyl aldosamines, N-acetylamino acids and related N-acetyl compounds and their topical use Compositions comprising N-acetyl-aldosamines, N-acetylamino acids, and related N-acetyl compounds are useful to alleviate or improve various cosmetic conditions and dermatological disorders, including changes or damage to skin, nail and hair associated with intrinsic aging and/or extrinsic aging, as well as changes or damage caused by extrinsic factors. N-acetyl-aldosamines, N-acetylamino acids, and related N-acetyl composition may further comprise a cosmetic, pharmaceutical or other topical agent to enhance or create synergetic effects.
EP2211858A2 Use of quaternary pyridinium salts for inhibiting cancer metastases The invention relates to a method for inhibiting and/or preventing formation of cancer metastases and secondary malignant cancers by administration to a subject of an effective amount of a quaternary pyridinium salt of formula (I) wherein R' is selected from the group consisting of H, OH, CONH2, and COCH3; R' is selected from the group consisting of H and CH3, R'' is selected from the group consisting of H and CH3; and X- is a pharmaceutically acceptable counterion.
WO2013148620A1 Benzofuran derivatives for the treatment of hepatitis c The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
WO2013142424A1 Beta-hydroxy-beta-methylbutyric acid for improving glucose tolerance The use beta-hydroxy-beta-methylbutyric acid for improving glucose tolerance in a pediatric individual or in an adult individual is disclosed. In certain embodiments, the beta-hydroxy-beta-methylbutyric acid is administered via a nutritional composition.
US8710095 Drugs for prophylaxis or mitigation of taxane-induced neurotoxicity Provided are pharmaceutical drugs for preventing or mitigating adverse actions associated with taxane antineoplastic drugs which are frequently and widely used in cancer chemotherapy, and pharmaceutical compositions which allow us to shorten the duration of treatment with taxane antineoplastic agents and/or to repeat the taxane treatment course more times, as well as drugs suitable for the therapeutic schedules.
CN101874783A Sustained-release preparation containing melatonin and preparation method thereof The invention discloses a sustained-release preparation containing melatonin and a preparation method thereof. The method comprises the following steps: preparing sustained-release pellets by the melatonin, wherein each sustained-release pellet comprises a celphere, a drug-loaded layer and a coating layer; and then, filling the prepared sustained-release pellets in capsules to prepare sustained-release capsules or pressing the pellets with proper auxiliary materials to form tablets. The preparation can better control sustained release of the medicament. Compared with the sustained-release tablets, the melatonin sustained-release preparation avoids the possible 'burst release' phenomenon of the sustained-release tablets; the pellets are uniformly distributed in a gastrointestinal tract to reduce irritation of the medicament to the gastrointestinal tract; the sustained-release preparation has small impact on food, and is suitable for special people, such as elders and children; and the preparation can be mixed with unit bodies with different releasing velocities to obtain preparations in accordance with different release requirements.
EP2624822A2 Allergen deactivator composition, articles and methods An allergen deactivator including a compound of the following Formula 1: wherein R represents a straight or branched chain alkyl group of C1 to C30, and X represents H, Na, K, Mg or Ca. Also disclosed is a spray, a filter, a fiber, a fabric, a nonwoven article, a substrate, and a detergent using the allergen deactivator including the compound of Formula 1.
US7029659 aqueous solvent, organic cosolvent, and occlusive agent, especially petrolatum, to form an occlusive layer on the skin for the topical administration of pharmaceuticals A topical mousse composition including an occlusive agent; an aqueous solvent; and an organic cosolvent, wherein the occlusive agent is present in an amount sufficient to form an occlusive layer on the skin.
WO2002065984A3 Compounds having retinoid-like activity There are provided compounds represented by formula (I) or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, wherein the various substituents are as defined. Also included are methods for preventing and/or treating tumors, arthritis, and non-malignant skin disorders comprising administering a compound of formula (I) to a mammal. Further provided are pharmaceutical formulations comprising a compound of formula (I) in admixture with one or more pharmaceutically acceptable excipients.
US20060233811 Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents The present invention is based on the discovery that the administration of at least one immunoconjugate and at least one chemotherapeutic agent provides an unexpectedly superior treatment for cancer. The present invention is directed to compositions comprising at least one immunoconjugate and at least one chemotherapeutic agent and to methods of treating cancer using at least one immunoconjugate and at least one chemotherapeutic agent. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one chemotherapeutic agent and at least one immunoconjugate.
CN101318950A Preparation method for couplet benzene ring octadiene system lignans and application thereof The invention provides a method for preparing dibenzocyclooctadiene lignan as shown in formula (I) and an application of the dibenzocyclooctadiene lignan on anti-HIV-1. The method has readily available raw materials, and simple and easy operation, and the prepared compound has remarkable anti-HIV-1 activity. R1=OH, R2=OCH3 or R1=OCH3.
US20120328653 Modified immunization vectors The disclosure relates to recombinant vectors and methods for using the same. In certain embodiments, the recombinant vectors are immunogenic.
US20120171151 Mass spectrometric quantitation assay for metabolites of leflunomide Methods are described for determining the amount of metabolites of leflunomide in a sample. More specifically, mass spectrometric methods are described for detecting and quantifying teriflunomide in a sample.
EP2732822A1 Therapeutic agent for bone fracture, bone growth enhancer, or therapeutic or prophylactic agent for bone diseases, each comprising carbon dioxide as active ingredient The present invention provides a prophylactic or therapeutic agent for fracture and bone diseases as well as a bone growth promoting agent containing carbon dioxide as an active ingredient. Further, according to the present invention, an additive or synergistic effect for preventing or treating fracture and bone diseases as well as for promoting bone growth by combining the therapeutic agent of the present invention and a bone absorption inhibitor and/or a bone formation promoter is obtained.
EP1933856A2 Method for treatment or prevention of conditions caused by gram-positive bacteria The treatment, prevention and prophylaxis of conditions such as sepsis, septic shock, systemic inflammatory response syndrome or 'SIRS', SIRS with organ dysfunction or failure, organ failure and organ dysfunction are described. These conditions are associated with infection by Gram-positive bacteria. The treatment involves the administration of compositions containing a phospholipid, a neutral lipid, and a bile acid or a bile acid salt.
US20090062327 Inhibitors of AKT Activity The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
EP2229943A1 Compounds for use in the treatment of peripheral neuropathy Benzodioxo compound (I) or its salt, is new. Benzodioxo compound of formula (I) or its salt, is new. A 1, A 2, A 3 : H, halo, or 1-4C alkyl group; R 1, R 2, R 3 : H, or 1-4C alkyl; Y 1 : -OH (preferred), (=O) or -SH; and n : 1 or 2. Independent claims are included for: (1) a pharmaceutical composition comprising (I) and at least an additional compound and/or at least one additional cytostatic or antimitotic compound and/or optionally in combination with a excipient; and (2) a products containing (I) and at least one additional compound and/or at least one additional cytostatic or antimitotic compound as a combination product for a simultaneous, separate or sequential use. [Image] - ACTIVITY : Neuroprotective; Antidiabetic; Antialcoholic; Nephrotropic. - MECHANISM OF ACTION : Gamma amino butyric acid receptor inhibitor; Cytochrome P1A2 isoenzyme inhibitor; Cytochrome P3A4 isoenzyme inhibitor.
CN101417971B Indolines compounds, preparation method and pharmaceutical application thereof The invention relates to the field of pharmaceutical chemistry, in particular to an alpha 1-AR antagonist indoline compound (I), wherein the definitions of R1, R2, R3 and m see the instruction. The invention also discloses a method for preparing the compound (I), a medical composition containing the compound (I), and application of the compound (I) in treating prostatoplasia and cardiovascular system diseases and adjusting the intraocular pressure.
EP2153825A1 Therapeutic formulation for administering tolterodine with controlled release The invention provides a pharmaceutical formulation containing tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine, or a pharmaceutically acceptable salt thereof, which formulation when administered to a patient provides controlled release of tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine, or a pharmaceutically acceptable salt thereof, such that a substantially constant serum level of the active moiety or moieties is maintained for at least 24 hours.
EP1888531A2 (5z)-5-(6-quinoxalinylmethylidene)-2-ý(2,6-dichlorophenyl)amino¨-1,3-thiazol-4(5h)-one Invented is the compound (5Z)-5-(6-quinoxalinylmethylidene)-2-[(2,6-dichlorophenyl)amino]-1,3-thiazol-4(5H)-one, and/or pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof. Also invented are pharmaceutical compositions containing this compound, methods of preparing this compound and pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof. Also invented are methods of using this compound as an inhibitor of hYAK3 proteins.
WO2007038314A2 Fused heterocyclic compounds useful as kinase modulators Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, and hydrates, thereof, (I) are useful as kinase modulators, including MK2 modulation, wherein one of E and F is a nitrogen atom and the other of E and F is a carbon atom, and Z is N or CR3, and R1, R2, R3, X and Y are as defined herein.
US20100211183 Chemical Mechanical Vapor Deposition Device for Production of Bone Substitute Material A method for fabricating a substitute component for bone, including the processes of: provision of a chemical spray including at least three of calcium chloride, hydrogen phosphate, hydrogen carbonate and water to form a combined solution; reaction and precipitation of the combined solution onto a substrate; allowing the precipitated particles to form a porous structure on the substrate; applying substantially isostatic pressure to the porous structure to form a compressed structure; and (optional) providing one or more through-holes in the compressed structure to promote osteoinduction.
US20090054448 Amino Acid Derivatives as Histone Deacetylase (HDAC) Inhibitors The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or stereoisomers thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.
CN102811724A Pharmaceutical composition having antimicrobial and fast-healing activity for external administration, process for preparing same This invention is related to pharmacology, medicine, veterinary science and pharmaceutical industry,in particular to the process for the production of original composite antimicrobial and vulnerary preparations for external administration having an increased therapeutic efficiency in the treatment of skin and soft tissues infections. The claimed pharmaceutical composition contains antibiotic fosfomycin and finely dispersed nanostructured silica dioxide as active agents. The claimed process for the production of the pharmaceutical composition consists in mixing fosfomycin substance with finely dispersed nanostructured silica dioxide, characterized in that the micture of said substances in the weight ratio (25-75% by weight) : (75-25% by weight) respectively is being exposed to mechanical treatment by impact and abrasive actions to increase the weight percentage of the finely dispersed fraction ( 5 micron) to at least 40%.
WO2011119748A1 Compositions comprising a prosamide for treating hair loss, hair thinning, hair color loss Described herein are compositions including at least one prostaglandin or prostamide and methods for using these compositions for increasing hair growth on the scalp eyebrow growth.
US7060826 Central nervous system disorders; Alzheimer's disease; huntington's disease; Parkinson's disease; attention deficit disorders; schizophrenia; Tourette's syndrome Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.
WO2004018465A9 Benzonaphthyridines with pde 3/4 inhibiting activity Compounds of a certain formula (1), in which R1, R2, R3, R4 and R5 have the meanings indicated in the description, are novel effective PDE4 or PDE3/4 inhibitors.
EP2570417A1 Thienopyridine ester derivative containing nitrile, preparation method, use and composition thereof A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation.
US20100098632 Hydroxyapatite particles This document provides methods and materials related to hydroxyapatite particles. For example, hydroxyapatite particles, methods for making hydroxyapatite particles, and methods for using hydroxyapatite particles are provided herein.
US20120329748 Activation and activators of sirt5 The invention provides a method of increasing a deacetylase activity of SIRT5 by contacting SIRT5 with an agent that binds SIRT5 and reduces the Km of SIRT5 for a substrate, thereby increasing the deacetylase activity of SIRT5. The invention also provides a method for treating a urea cycle disorder in a mammal, as well as a method of assaying a sirtuin modulator.
US20090182055 Fungicidal agent containing n-chlorotaurine and use thereof A fungicidal agent for treating infectious diseases caused by fungi contains N-chlorotaurine or one of its salts in aqueous solution, optionally with customary pharmaceutical additives.
CN1771960A Dimenhydrinate dripping pill and its prepn The present invention discloses one kind of dimenhydrinate dripping pill and its preparation process. The dimenhydrinate dripping pill is compounded with dimenhydrinate and dripping pill matrix. The present invention has high bioavailability, high stability, convenient taking, fast disintegration and dissolving, high leaching degree, fast medicine releasing, fast acting, simple production process, low cost and other features.
CN103570665A Enantiomers of 3-methyl-7, 8-dihydroxy-isochroman-4-one, and applications thereof in controlling cardiovascular diseases The invention belongs to the field of organic chemistry and pharmaceutical chemistry, and specifically relates to a levorotatory enantiomer and a dextrorotatory enantiomer of a natural product 3-methyl-7, 8-dihydroxy-isochroman-4-one (XJP), a preparation method thereof, and applications of the levorotatory enantiomer and the dextrorotatory enantiomer in controlling cardiovascular diseases.
WO2009037538A3 Process for the preparation of lamivudine form i The present invention provides a process for preparing a stable crystalline solid of Lamivudine polymorphic Form I, which does not change to Form II during storage and pharmaceutical unit operations.
US20110117223 Antiseptics The present invention is based on the surprising antiseptic nature of chlorhexidine when combined with essential oils. It has been found that chlorhexidine, combined with an essential oil, is surprisingly effective at penetrating the skin surface and providing an antiseptic effect within the skin. It has also been found that a combination of chlorhexidine and eucalyptus oil is surprisingly effective as an antimicrobial against Staphylococcus epidermidis.
WO2007062877A3 PRODRUG ERβ-SELECTIVE SUBSTANCES, METHODS FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS The invention relates to a prodrugs of 9α-substituted estratrienes of general formula (I), wherein the Z group is linked to a steroid, (I). The invention also relates to a methods for the production thereof, pharmaceutical compositions which contain said compounds, and to the use thereof. Said inventive compounds of general formula (I) do not bond with the oestrogen receptor alpha and/ or beta but they bond with carboanhydrases and inhibitors of said enzymes.
CN101961337A Medicinal composition with aciclovir sodium as active ingredient The invention relates to a medicinal composition with aciclovir sodium as an active ingredient. The medicinal composition comprises aciclovir sodium shown by the following structure or a hydrate thereof, wherein the chemical name is 9-(2-hydroxyethoxymethyl) sodium guanine; and the medicinal composition is prepared from the aciclovir sodium and pharmaceutically acceptable auxiliary materials by preparation technology.
CN101273972A Method for preparing magnetic adriamycin poly-alkyl-alfa-cyanoacrylate nanoparticles The invention discloses a preparation method of magnetic doxorubicin polybutylcyanoacrylate nanoparticles, which relates to the preparation of osteosarcoma targeted therapeutic nanodrugs. The magnetic doxorubicin polybutylcyanoacrylate nanoparticles are mainly prepared by Fe3O4 water-based magnetic fluid, Dextran-70, Tween80, doxorubicin hydrochloride, Alpha-polybutylcyanoacrylate and so on. The ADM-PBCA-MNPS prepared by the invention is a novel targeted drug delivery system-magnetic targeted drug delivery system, which has the advantages of simple preparation method, lower production cost, good targeted effect, easy implementation of targeted therapy and so on, thus showing great application prospect in the field of the targeted therapy of tumors.
WO2010003308A1 The use of nitric oxide and signal transduction system thereof in preparing medicaments for targeted therapy of malignant tumors The use of nitric oxide and signal transduction system thereof in preparing the medicaments for targeted therapy of malignant tumors. The medicaments are selected from targeted medicaments which can alter expression or activity of inducible NOS, endothelial NOS and neural NOS and so forth.
CN1830976A Extractive of total benzofuran of benzoin plants, prepn. method and use thereof A general benzifuran is extracted from the Styrax plant and can be used to prepared injection, tablet, capsule, etc for preventing and treating early failure of ovary function, climacteric syndrome, osteoporosis, polycystic overy syndrome, acyesis, etc. Its preparing process is also disclosed.
CN103694303A Antitumor compound extracted from guttifer, and preparation method and application thereof The invention relates to an antitumor compound extracted from guttifer, and a preparation method and application thereof. The preparation method of the compound comprises the following steps: (1) taking the medicinal material guttifer, extracting with ethyl acetate, carrying out silica gel column chromatographic separation on the extract, and carrying out petroleum ether-ethyl acetate gradient elution to obtain 11 components A-K; (2) discarding the grease components and garcinia acid components, carrying out HPLC-PDA-MS (high performance liquid chromatography-potato dextrose agar-Murashige-Skoog) repeat analysis to obtain a key component I; (3) carrying out silica gel column chromatographic separation on the component I, and carrying out chloroform-methanol gradient elution to obtain a fraction I-2; (4) carrying out silica gel chromatographic separation on I-2, and carrying out chloroform-methanol gradient elution to obtain a subfraction I-2A; and (5) carrying out reversed phase RP-18 separation and acetonitrile-water gradient elution on the I-2A to obtain the compound. The compound can be used for treating tumors.
US7022696 Treatment of airway disorders The compounds of formula I in which R1, R2, R3, A, X, s and R9 have the meanings as given in the description are novel effective PDE4 inhibitors.
CN103417914A TCM composition for treatment of acute renal failure The invention discloses TCM composition for treatment of acute renal failure. The TCM composition comprises the raw material medicines of 25-150 g of gypsum, 12-25 g of rhizoma anemarrhenae, 15-30 g of root of rehmannia, 10-25 g of honeysuckle, 10-12 g of radix achyranthis bidentatae, 12-18 g of gardenia jasminoides ellis, 10-18 g of salvia miltiorrhiza, 10-15 g of radix curcumae, 12-18 g of ligusticum wallichii and 10-15 g of root of common peony by weight. According to the invention, years of research and clinical observation of hundreds of patients show that the TCM composition for treatment of acute renal failure has an obvious clinical treatment effect. The positive effect against the renal failure is achieved, and the TCM composition has the curative effects of improving the renal function, reducing urea nitrogen and creatinine, and the like, and has the efficacies of clearing heat, removing toxicity, draining turbidity to save the renal, relieving stagnant qi and cleaning abdominal mass, cooling blood and hemostasis, engendering liquid and dredging collaterals, increasing humor and offensively precipitating, and the like.
WO2007116149A1 Novel strontium salts of sulfonic acids, process for preparing them and the pharmaceutical compositions containing them Strontium salts of the sulfonic acids of formula (I): A-B-SO3H (I) in which: A is a group chosen from OH, NH2, SO3H and CO2H, and B is an arylene group or a linear or branched C1-C12 alkylene chain which is optionally substituted and in which one or more of the carbon atoms is optionally replaced with an oxygen or nitrogen atom or an SO2 group. Medicaments.
CN1895237A Officinal magnolia phenol lipid frozen dried powder preparation and its use in preparing drug for cancers A freeze-dried powder of honokiol liposome for preparing the medicines to treat lung cancer and mammary cancer is proportionally prepared from honokiol, polyethanediol-phosphatidylethanolamine, lecithin and cholesterol. It has high synergistic and sensitizing action when it is applied in conjunction with chemicotherapeutic medicine.
US20100092496 drug-ligand conjugates that are potent cytotoxins; stabilized therapeutic agents and markers; exhibit high specificity of action, reduced toxicity, and improved stability in blood ; antitumors The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.
WO2010105372A1 Compositions and methods for silencing hepatitis c virus expression The present invention provides compositions comprising therapeutic nucleic acids such as interfering RNA that target hepatitis C virus (HCV) gene expression, lipid particles comprising one or more (e.g., a cocktail) of the therapeutic nucleic acids, methods of making the lipid particles, and methods of delivering and/or administering the lipid particles (e.g., for the treatment of acute or chronic hepatitis C caused by one or more HCV genotypes).
EP1257270B1 A method for synthesizing leflunomide A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided. Further provided is the leflunomide prepared by the inventive process, which is substantially free of difficult-to-separate impurities often found in leflunomide prepared by known methods, including N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 5-methyl-N-(4-methylphenyl)-isoxazole-4-carboxamide and N-(4-trifluoromethylphenyl)-3-methyl-isoxazole-4-carboxamide. The invention further provides pharmaceutical compositions and dosage forms containing highly pure leflunomide and methods of treating disease using the leflunomide.
WO2004106279A3 CRYSTALLINE FORM OF β2 ADRENERGIC RECEPTOR AGONIST The invention provides a novel β2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel β2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with β2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.
EP2468303A1 Functionalized nucleic acids and particles comprising them for the treatment of HIV infections The present invention relates to a particle comprising a functionalized nucleic acid non-covalently associated to a cell-penetrating peptide, wherein: • the functionalized nucleic acid comprises, or consists of: - an HIV integrase-inhibiting oligonucleotide comprising from 11 to 20 contiguous nucleotides; and - at least one functionalizing group of the following formula (I) covalently linked to the oligonucleotide: • the cell-penetrating peptide comprises from 12 to 30 contiguous amino acids; • the particle is liable to be obtained by contacting the functionalized nucleic acid with the cell-penetrating peptide in a 1/5 to 1/15 molar ratio.
WO2013057253A1 Pyrimidin-4-one derivatives and their use in the treatment, amelioration or prevention of a viral disease The present invention relates to a compound having the general formula (II), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, Formula (II) which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
CN101648973B Water-soluble taxane and preparation method thereof The invention provides water-soluble taxane which comprises water-soluble four-ring taxane, water-soluble five-ring taxane and water-soluble six-ring taxane. Taxane (a) reacts with the formula (1) under the existence of alkali to obtain ester (b) of which the second site or the seventh site or the second site and the seventh site are substituted; and the (b) reacts with the reaction to obtain a target product. The water-soluble taxane has favorable water solubility and can be directly made into powder injection or transfusion without adding a surface active agent and an oily auxiliary material during preparation, can be also made into oral preparation because of favorable bioavailability, and can be used for preparing a treating medicine for clinically treating tumor patients. On one hand, the water-soluble taxane is convenient for clinical application, on the other hand, the compliance of the patients is improved, thereby having obvious advantages and market value. The structural formula is shown as the formula (I).
EP2077260A1 Amide compound or salt thereof, and biofilm formation inhibitor, biofilm remover and bactericide each using the amide compound or salt thereof The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilm. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.
EP1326586B1 New pharmaceutical compositions containing epinastine and pseudoephedrine The present invention relates to novel oral pharmaceutical compositions comprising as pharmaceutically active compounds a combination of an antihistaminic-effective amount of epinastine or a pharmaceutically acceptable salt thereof and of a decongestant-effective amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and further comprising suitable pharmaceutically acceptable carriers or excipients. The invention further relates to methods for the preparation these compositions and methods of using them in the treatment of allergic diseases and/or disorders.
EP1230925B1 Use of a trifluridine derivative alone or combined with a thymidine phosphorylase inhibitor for the treatment of hiv An anti-HIV composition containing at least one member selected from the group consisting of trifluridine and derivatives thereof and a pharmaceutically acceptable carrier; an anti-HIV composition containing as the active ingredients (a) at least one member selected from the group consisting of trifluridine and derivatives thereof, (b) a thymidine phosphorylase inhibitor, and a pharmaceutically acceptable carrier; and a composition for potentiating the anti-HIV activity of trifluridine or derivatives thereof, containing a thymidine phosphorylase inhibitor and a pharmaceutically acceptable carrier.
CN1861092A Application of chlorine-contg. disinfectant in pharmaceutics An application of the chlorine contained disinfectant in preparing medicines for treating beriberi and tines pedis is disclosed.
US20110281813 Method of treating c-kit positive relapsed acute myeloid leukemia The present invention relates to a method of treating c-kit positive relapsed acute myeloid leukemia (AML) in a human patient population using a combination comprising a c-kit inhibitor, daunorubicin and cytarabine.
EP1595878A1 Indole derivatives with apoptosis inducing activity N-(2-(1-Substituted 1H-indol-3-yl)-2-oxo-acety l)-N-heterocyclyl-amide or -carbamate compounds (I) are new. - Indole derivatives of formula (I) and their tautomers, stereoisomers (including diastereomers and enantiomers) and salts are new. - R = optionally substituted saturated, unsaturated or aromatic 2-14C heterocycle, containing one or more of N, O and/or S as heteroatom(s); - R1 = optionally substituted alkyl-aryl; - R2 = H or optionally substituted 1-6C alkyl; - R3 - R6 = H, optionally substituted 1-6C alkyl, optionally substituted 3-7C alkyl, NH2, mono- or di-(1-4C) alkylamino, halo, 1-4C mono- or polyfluoroalkyl (specifically CF3), CN, cyano-(1-6C) alkyl, (1-6C) alkylcarbonyl, COOH, (1-4C) alkoxycarbonyl, carboxy-(1-6C) alkyl, (1-6C) alkoxycarbonyl-(1-6C) alkyl, OH, 1-6C alkoxy, aryl-(1-4C) alkoxy (preferably OCH2Ph), (1-6C) alkoxycarbonylamino or (1-6C) alkoxycarbonylamino-(1-6C) alkyl; - R7 = (1-6C) alkylcarbonyl or (1-6C) alkoxycarbonyl; - X, Y = O or S; - Provided that if R = optionally substituted pyridyl, then R7 is not acetyl or tert. butoxycarbonyl. - ACTIVITY - Cytostatic. - In tests in a human xenograft model in mice, oral administration of N-(2-(1-(4-chlorobenzyl)-1H-indol-3-yl)-2-oxo-acetyl)-N-quinolin-6-yl -acetamide (Ia) at 80 mg/kg p.o. caused complete remission in 6/6 mice with transplanted MEXF462 melanoma and was well tolerated. - MECHANISM OF ACTION - Tubulin polymerase inhibitor; topoisomerase II inhibitor; apoptosis inhibitor.
CN103638258A Composition for tonifying spleen and nourishing stomach The invention relates to a composition for tonifying spleen and nourishing stomach. The composition is prepared from the following components in parts by weight: 45-55 parts of smoke plum, 15-25 parts of fig, 15-25 parts of semen raphani, 15-25 parts of poria, 10-20 parts of striga asiatica, 20-30 parts of lotus seed, 20-30 parts of yam, 3 parts of vitamin C and 3 parts of vitamin B. The method for preparing the composition comprises the following steps: weighing the components in the ratio; crushing all the components into 1,000 meshes; adding the crushed components, except vitamin C and vitamin B, into 300 parts by weight of water, and boiling for 30 minutes; concentrating to thick paste, cooling, adding the vitamin C and the vitamin B, and uniformly stirring to prepare pills. The composition for tonifying spleen and nourishing stomach is scientific in prescription, reasonable in dosage and easy to absorb, metabolism can be promoted, and functions of spleen and stomach can be strengthened.
US20080114038 Drugs Derived from Diclofenac Containing No-Donor Heterocycles, Composition and Method of Inflammation Treatment The present invention refers to drugs resulting from the pharmaceutical substance diclofenac, relative to the formula. The invention further refers to a pharmaceutical composition, which involves the said drugs and a pharmaceutically adequate vehicle. It is also described a method for the treatment of inflammation through the administration of the new drugs in patients with gastric problems or subjected to long-term treatments.
WO2012153729A1 Heteroaromatic ring derivative The compound represented by formula (IA) or a pharmaceutically acceptable salt thereof is based on orexin (OX)receptor antagonist activity, is useful in the treatment and prevention of illnesses including sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependency, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, pain, gastrointestinal disease, epilepsy, inflammation, immunological disease, endocrinological related disease, and hypertension.
US20070149587 Valsartan Salts The invention relates to new salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.
US20060105988 Antipruritic composition for external use on skin It is the object of the present invention to provide a composition which has an antipruritic effect on skin and further exhibits good appearance and feeling of usage. The present invention relates to an antipruritic composition for external use on skin, which contains a mucopolysaccharide or a derivative thereof in an amount of 0.5 to 20 weight %.
CN1813733A Vitamin E nicotinate lipide microsphere injection and its preparing method The present invention provides a lipid microsphere injection containing vitamin E nicotinate and its preparation method. The invented preparation utilizes the interfacial membrane medicine-carrying principle to greatly raise medicine-carrying quantity and stability of water-insoluble medicine vitamin E nicotinate in the emulsion and reduce its toxicity, and raise its target property and patientí»s compliance. The distributed quantity of the invented vitamin E nicotinate in the interfacial membrane of oil-water two phases and oil phase can be up to 80-98%. Said preparation can be used as a new preparation for reducing blood-lipid.
WO2007079169A2 Treatment for acute myeloid leukemia The present invention provides a method of treating acute myeloid leukemia. Generally, the method includes administering to a patient with AML an amount of a TLR agonist compound effective to decrease the percentage of leukemic cells in the patient's peripheral blood or bone marrow.
CN102895586A Preparation method of medicinal powder containing costus root and amomun cardamun for treating dysphagia The invention relates to a preparation method of a medicinal powder containing costus root and amomun cardamun for treating dysphagia. The method comprises the steps of: peeling amomun cardamom; drying costus root and darkdried plum; grinding the medicines with borax into a superfine powder; then pouring honey into a pan and decocting to a yellowish state; pouring the powder into the pot; and stirring well and preparing into honeyed pills. The product is convenient for administration, and shows quite obvious effects on dysphagia, caused by vomiting after meal, hiccup and sputum obstruction.
WO2013015714A1 Method for treating chronic viral hepatitis c The invention relates to medicine, more specifically hepatology, and can be used for treating chronic viral hepatitis C, the causative agent of which can be of any genotype. The technical result of the proposed method is a reduction in the aggressiveness of antiviral therapy together with an increase in stable positive therapeutic results. In the claimed method for treating chronic viral hepatitis C, which involves administering short-lived interferon-alpha (IFN) and the nucleoside analogue Ribamidil to the patient, an average weekly starting dose of interferons in a range of 10.5-21.0 million SU is determined on the basis of the patient's own interferon-alpha level, and interferon-alpha is administered with an at least twofold gradual increase in the average weekly dose of interferons to a value of 21.0-84 million SU. Throughout the entire IFN administration period, additional antiviral drugs, namely an interferon inducer, are administered to the patient, as well as an amantadine group preparation or a glycyrrhizic acid preparation. At the same time, a concomitant treatment is carried out which involves the administration of T cell immunity stimulators and preparations for combating side effects. The presence of viral ribonucleic acid (RNA) in the patient's blood is periodically monitored: a daily dose of 800-1200 mg of Ribamidil is administered starting from the third month from the commencement of treatment if ribonucleic acid (RNA) is present in the patient's blood, or starting from the tenth month if no RNA is present. Treatment is continued until at least a twelve month period of aviremia has passed.
CN102793821A Pills comprising sanguisorba officinalis, frankincense, rhizoma corydalis and myrrh The invention discloses pills comprising sanguisorba officinalis, frankincense, rhizoma corydalis and myrrh, and belongs to a latest product invented at present. Gout is a disease caused by the reason that uric acid is excessive and difficult to discharge, and the disease has main symptoms that the joint at a sick part protrudes, swells and aches, the halluces joint aches at the beginning, a certain part of the foot joint such as toes, ankles and wrists may ache and the elbow joint aches in succession; and the ache can continue for two to three days or longer and attack continually, so that patients are subjected to great pain. The pills consist of sanguisorba officinalis, frankincense, rhizoma corydalis, myrrh, nutgrass galingale rhizome, potassium and baking soda. The pills can diminish inflammation, relieve pain, dissipate blood stasis, dredge stasis, diminish swelling and induce diuresis, and have a remarkable treatment effect on gout patients.
EP1545579A1 Compositions containing peptide copper complexes and phytochemical compounds, and methods related thereto Novel compositions having anti-oxidant, anti-inflammatory and/or cosmetic utility for a mammal, combine at least one peptide copper complex and at least one phytochemical compound. More particularly, disclosed are such novel compositions where the phytochemical compound is a polyphenol or a carotenoid, the polyphenol being a flavanoid, a flavonoid, a flavonoid derivative, a flavolignan, a polyphenolic rhizome, or a mixture thereof. Compositions for topical application are disclosed that include additives such as emollients, sunscreen agents, skin protectants, skin conditioning agents, and humectants. Also disclosed are methods, employing such compositions, for enhancing or restoring the resistance of a mammal to oxidative or inflammatory damage, for accelerating wound healing, for cosmetically healing mammalian skin, and for stimulating hair growth, or preventing or treating hair loss.
US20110123448 Oil body carriers, uses in target therapy and/or detection of the same, and fusion proteins comprised therein An oil body carrier, its uses in target therapy and/or detection, and a fusion protein comprised therein are provided. The oil body carrier comprises: a) the fusion protein, comprising an oil body protein and a ligand peptide, an antibody peptide, a cell penetrating peptide, or combinations thereof, and b) a lipid, wherein the weight/volume (μg/μl) ratio of the fusion protein and the lipid is at least about 1/25, and the average particle size of the oil body carrier is about 10 nm to about 2,000 nm.
WO2008087123A2 Use of 5-ht6 antagonists to prevent relapse into addiction The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are 5-HT6 antagonists. These compounds are useful for the preparation of medicaments for preventing relapse into addiction, in particular relapse into addiction to substances of abuse, including opiates, hallucinogens, inhalants, phencyclidine, amphetamines, cocaine, cannabis, nicotine, and alcohol, into relapse to addiction to certain medicines, including sedatives, hypnotics and anxiolytics, and into relapse to certain addictive behaviors, including gambling.
CN101519402A Thiochromone compound, synthetic method and application thereof in preparing antifungal medicaments The invention relates to a thiochromone compound, which has the structure as right: wherein R1 is five-membered nitrogen-containing aromatic heterocycle substituted by hydrogen, methyl, nitryl or cyano; R2 is aliphatic alkyl of C1 to C12 or unsubstituted five-membered or six-membered aromatic ring aliphatic alkyl or five-membered or six-membered aromatic ring aliphatic alkyl selectively substituted by amino group, methyl, trifluoromethyl, trifluoromethoxy, nitryl, halogen and cyano; R3 is alkyl, hydrogen, fluorine, chlorine, bromine or iodine of C1 to C4; R4 is hydrogen, fluorine, chlorine, bromine, iodine or five-membered or six-membered heterocycle containing nitrogen; and R5 and R6 are hydrogen, fluorine, chlorine, bromine, iodine, alkyl of C1 to C4, hydroxyl, oxyl of C1 to C4, cyano, nitryl, amino group or amino group substituted by alkyl of C1 to C4. The compound has application in preparing antifungal medicaments, strong bacteriostatic activity for common pathogenic fungus and deep fungal infection, low toxicity, good stability and broad antifungal spectrum.
US20120071440 Pharmaceutical Composition For Enhancing Adiponectin Production And Food Useful Therefor A pharmaceutical product having excellent adiponectin production ability, and food useful for the pharmaceutical product is provided. The pharmaceutical product contains, as active ingredients, a sugar having a polymerization degree of 2-10, wherein mannose units account for not less than 50% based on the number, and a chlorogenic acid.
CN1730034A Pharmaceutical composition for treating acute pneumonia, urinary tract infection and cholecystitis The invention relates to a medicinal composition for treating acute pneumonia, urinary tract infection and cholecystitis, as well as the process for preparation, more specifically, the invention relates to a medicinal composition of baikal skullcap root extract and fibraurea stem extract and the preparing process.
US7763601 Using O-(3-piperidino-2-hydroxypropyl)-nicotinic amidoxime (BGP-15); weight loss O-(3-piperidino-2-hydroxypropyl)-nicotinic amidoxime (BGP-15) or a pharmaceutically suitable acid addition salt thereof can be used for the prevention or reduction of weight gain or the reduction of the rate of body weight gain.
US20060293239 Treatment and Diagnosis of Insulin-Resistant States Dickkopf-5 (Dkk-5) protein is administered in effective amounts to treat disorders involving insulin resistance, such as non-insulin-dependent diabetes mellitus (NIDDM) or obesity. Also provided is a method of diagnosing insulin resistance and related disorders using Dkk-5 as a measure, and kits for diagnosis and treatment, as well as hybridomas producing antibodies to Dkk-5 and preparations comprising Dkk-5.
US20070160657 Targeting and intestinal-absorption controlled liposome having sugar chain and therapeutic drug for cancer and diagnostic drug containing the liposome An object of the present invention is to provide a liposome having a sugar chain bonded thereto, the sugar chain having an activity of specifically binding to various lectins (sugar chain recognizing proteins) present on the cell surfaces of various tissues and thus being capable of actually distinguishing a cell and a tissue in vivo, thereby efficiently delivering a medicinal drug or a gene.
WO2008119719A1 1- (1-cyclohexyl-4-piperidinyl) -1, 3-dihydro-2h-benzimidazol-2-one derivatives which have activity on the m1 receptor and their use in medicine Compounds of formula (I) or a salt thereof are provided, wherein R4, R5, R6, Q, R1 and R2 are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
WO2010070343A1 1,3,4-oxadiazole derivatives and their uses to treat diabetes DGAT-1 inhibitor compounds of formula (I) and pharmaceutically-acceptable salts thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity (I) wherein n is 0, 1, 2 or 3, R is independently selected from fluoro, chloro, bromo, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy and Z is carboxy or a mimic or bioisostere thereof, hydroxyl, hydroxymethyl, or −CONRbRc wherein Rb and Rc are independently selected from hydrogen and (1-4C)alkyl, which (1-4C)alkyl group may be optionally substituted by carboxy or a mimic or bioisostere thereof.
US20130004460 Silylated biomolecules The invention concerns: a silylated biomolecule having the following formula (I): the process for the preparation of a silylated biomolecule of formula (I), the use of a silylated biomolecule of formula (I) to functionalize the surface of a support, a process for the preparation of a hydrogel by use of a silylated biomolecule of formula (I), the hydrogel obtainable by said process, said hydrogel as a biological tissue substitute, a composition comprising said hydrogel in a pharmaceutically acceptable vehicle, said composition for the release of active principle.
CN101015540A Refreshing eyedrop and its preparation The invention provides an eye drop for eye care, wherein the constituents include chlorhexidine gluconate 0.01-8%, taurine 0.01-5%, sorbitol (70%) 0.1-18%, methyl glycol 0.1-28%, menthol 0.001-8%, ethanol 0.01-20% and right amount of purifying water. The preparing process consists of proportioning raw materials according to formulation quantity, dissolving menthol with ethanol into alcoholic solution, charging other raw materials into container, charging into pure water, obtaining water solution through sufficient dissolving, charging menthol alcoholic solution into water solution, stirring homogeneously, filtering and split charging.
US20110268718 Cactus fruit extract A method for producing a cactus fruit extract for use in formulating a beverage which can be used in the treatment of veisalgia.
US20080081800 2-Methylene-(20R,25S)-19,27-Dinor-(22E)-Vitamin D Analogs This invention discloses 2-methylene-(20R,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20R,25S)-19,27-dinor-(22E)-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
US20060199840 Chemical derivatives and their application as antitelomerase agent The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans.
WO2006077851A1 Quinolone derivative and salt thereof Disclosed is a compound having an excellent platelet agglutination inhibitory effect. Specifically disclosed is a quinolone derivative characterized by having an amide group at the 3-position which is substituted with a substituent having a carboxylate ester, phosphate ester, sulfate ester or the like, and an amino group at the 7-position which is substituted with a substituent having a ring structure. Also disclosed is a pharmaceutically acceptable salt of such a quinolone derivative. The quinolone derivative and a pharmaceutically acceptable salt thereof have excellent P2Y12 inhibitory effect and platelet agglutination inhibitory effect. Consequently the quinolone derivative and a pharmaceutically acceptable salt thereof are useful as a platelet agglutination inhibitor.
CN102020540B Three protein tyrosine phosphatase 1B (PTP1B) inhibitors and synthesis and application thereof The invention relates to a chemical complete synthesis method for three novel PTP1B inhibitors and application of the PTP1B inhibitors in medicines for treating type II diabetes. The chemical structural formulas of the PTP1B inhibitors are shown as follows: a compound 6 (4, 5-di-(2, 3-dibromo-4, 5-dimethoxybenzyl)-1, 2-dimethoxyphenyl): groups connected with C of 2', 3', 2'' and 3'' sites of a benzene ring are bromine atoms, and C of 1, 2, 4', 5', 4'' and 5' sites is connected with methoxyl; a compound 7 (3-bromo-4, 5-di-(2, 3-dibromo-4, 5-dimethoxybenzyl)-1): the groups connected with C of 3, 2', 3', 2'' and 3'' sites of the benzene ring are bromine atoms, and C of 1, 2, 4', 5', 4'' and 5' sites is connected with the methoxyl; and a compound 8 (3-bromo-4, 5-di-(2, 3-dibromo-4, 5-dyhydroxylbenzyl)-1, 2-dihydroxybenzene): the groups connected with C of 3, 2', 3', 2'' and 3'' sites of the benzene ring are bromine atoms, and C of 1, 2, 4', 5', 4'' and 5'' is connected with hydroxyl. The three compounds enhance the sensitivity of an insulin receptor through inhibiting the activity of protein tyrosine phosphatase 1B and have good therapeutic action on insulin resistant type II diabetes.
US20100068695 Inhibitor for enzyme having two divalent metal ions as active center A pharmaceutical composition for use as an inhibitor of an enzyme having two divalent metal ions as an active center was found. It is possible to inhibit the activity of an enzyme by a compound capable of chelating both of the two divalent metal ions.
CN1853640B Doxycycline hyclate liposome and production thereof A doxycycline hydrochloride liposome with high optical and thermal stability, high power to pass through skin and mucosa, and high antibacterial effect is prepared from phosphatide, cholesterol, doxycycline hydrochloride and emulsifier by film dispersing method, injection method, or reverse evaporation method.
US6942861 Functional bacterial protein, intimin, and its use as an antigen for protecting against infection by or transmission of bacteria expressing intimin-like proteins, such as certain pathogenic strains of Escherichial coli The present invention describes the isolation and purification of histidine-tagged functional portions of intimin (his-tagged intimin or his-intimin), a protein associated with the ability of certain strains of pathogenic bacteria to adhere to epithelial cells. The invention further describes the use of intimin as an antigen to promote a protective immune response. In addition, the invention describes the combination of intimin with one or more other antigens and administration of the combination to promote a protective immune response against intimin and the one or more antigens. One aspect of the invention is the administration of intimin to target specific epithelial cells to promote a protective immune response to intimin proteins. Additional aspects of the invention include the use of intimin or intimin combined with one or more antigens and administration of the combination to target gastrointestinal mucosa and stimulate an immune response. Additionally, the invention describes administration of the combination of intimin combined with drugs, to provide a means for targeted delivery of drugs to specific epithelial cells. Other aspects of the invention include the production of antibodies directed against his-intimin and methods of using such antibodies to provide passive immune protection, and in an assay system.
WO2012151141A3 A facile preparation of 4-substituted quinazolines and related heterocycles A straightforward single step method for the preparation and/or production of substituted quinazolines is disclosed, wherein said quinazolines preferably contain one substituent at position 4, and may contain other functional groups at various positions, such as 5, 6, 7, and/or 8 of quinazolines. In addition, the extension of this new method leads to the formation of different type of heterocyclic aromatic compounds, that include but are not limited to perimidines, anthrapyrimidin-7-ones (also known as anthrapyrimidinones), anthra[1,9:5, 10]dipyrimidines (also known as quinazoline[5,4-ef]perimidines) and benzo[e]- pyrimido[4,5,6-gh]pyrimidines.
US20110300247 Flaxseed lignan complex and its use thereof The invention relates compositions and methods for treating pathological lung conditions using whole-grain flaxseed or flaxseed lignans. Specifically, the invention relates to the dietary use of flaxseed lignans.
CN101810582A Method for preparing veterinary tilmicosin microspheres The invention discloses a method for preparing veterinary tilmicosin microspheres, which prepares the microspheres by using glucosan to encapsulate a tilmicosin medicament and comprises the following steps of: firstly, preparing a water phase containing the glucosan and tilmicosin and an oil phase containing an emulsifying agent, and mixing the water phase and the oil phase uniformly at the temperature of between 55 and 65 DEG C; secondly, reducing the temperature of the mixed solution to between 5 and 10 DEG C; thirdly, adding a dehydrating agent into the mixed solution; and finally, stirring and filtering the mixture to obtain uncrosslinked microspheres, and performing crosslinking on the microspheres in a crosslinking agent to obtain the tilmicosin microspheres. The tilmicosin microspheres prepared by the method are mainly centralized at the lung in an animal body after being taken, have very good targeting performance, can treat bacterial infections at the lung of an animal, and have a very good curative effect; besides, the preparation method is simple, has low energy consumption, small toxicity and high safety and needs no special equipment, and the finally-prepared tilmicosin microspheres have high encapsulation efficiency and low preparation cost, and are suitable for mass production.
WO2014014314A1 Hetrocyclic derivative having dual inhibitory activity A hetrocyclic derivative, having the structure expressed by chemical formula 1, and pharmaceutically acceptable salts, isomers, hydrates, or solvates thereof inhibit apoptosis-resistant proteins and protein kinases simultaneously, and have few side effects, and thus a pharmaceutical composition containing same is selective for diseases with abnormal cell growth caused by excessive activities of apoptosis-resistant proteins and protein kinases, and can be used as an efficacious preventative or therapeutic agent.
CN102805874A Anal fistula ultrasound contrast liquor The invention provides novel anal fistula ultrasound contrast liquor. The contrast liquor comprises the ingredients as follows: 0.1-0.5% of hydrogen peroxide solution : 0.05-0.5% lidocaine = 5:2 (v/v). The contrast liquor also comprises methylene blue solution. The anal fistula ultrasound contrast liquor disclosed by the invention enhances the ultrasound contrast inside the rectum cavity, has obviously higher accuracy rate than a conventional ultrasound for diagnosing the internal orifice and the primary tributary canal of the complex anal fistula, can provide more accurate anatomical morphology and position description for clinic, and basically cause no pain to patients during check.
WO2007042885A3 Therapeutic combination comprising methotrexate and a specified inhibitor of mek1 and mek2 The present invention relates to a method of treating rheumatoid arthritis with a combination, consisting essentially of N-[4-[[(2,4-diamino-6- pteridinyl)methyl]methylamino]benzoyl]-L-glutamic acid, or a pharmaceutically acceptable salt thereof, and N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and related combinations and pharmaceutical compositions.
EP1482951B8 1-alpha-hydroxy-2-methylene-19-nor-pregnacalciferol and its uses This invention discloses 1 alpha -a-hydroxy-2-methylene-19-nor-pregnacalciferol and pharamaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkels, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any calcemic activity and therefore may be used to treat immune disorders in humans as well as renal osteodystrophy.
US6977254 For prevention and/or suppression of preterm labor, suppression labor at term prior to caesarean deliver, and for the treatment of dysmenorrhea, useful in enhancing fertility rates The present invention provides substituted 10,11-Dihydro-5H-benzo[e]-pyrrolo[1,2-a][1,4]diazepine and 9,10-Dihydro-4H-3a,5,9-triaza-benzo[f]azulene compounds as well as methods and pharmaceutical compositions utilizing these compounds for the treatment and/or prevention and/or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and/or suppression of preterm labor, suppression labor at term prior to caesarean deliver, and for the treatment of dysmenorrhea. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals.
CN101856452A Medicament for treating bronchitis and preparation method thereof The invention discloses a medicament for treating bronchitis, which is prepared from the following raw materials: fried ephedra herb, apricot kernel, gypsum, scutellaria laterifolia, the root bark of white mulberry, the root of balloonflower, yedoensis, the rhizome of Chinese goldthread, dahurian patrinia herb, radishseed, fried coltsfoot, snakegourd fruit, aster, loquat leaf, bryozoatum, airpotato yam rhizome and liquorice. The medicament can be prepared into a variety of medicaments for clinical use, and has the effects of ventilating lung and relieving exterior syndrome, and reducing heat and curing asthma, and has good treatment effect on the bronchitis caused by various reasons. The medicament for treating the bronchitis has the advantages of quick response, high effective rate, no toxic or side effects, and safe and reliable clinical application.
US20110165266 Screen for inhibitors of hiv replication A method of screening test chemicals or compounds as inhibitors of HIV replication is disclosed. In one embodiment, the method comprises the step of determining whether the test chemical or compound is a sulfonation inhibitor. In another embodiment, the invention is a method of treating an HIV infected individual to reduce HIV replication comprising the step of treating the individual with an effective amount of sulfonation inhibitor.
US7470436 Water-soluble composition containing coenzyme Q10 A water-soluble composition comprising (A) coenzyme Q10 of 5-40% by weight, (B) monoester of polyglycerol with average polymerization degree of 10 and fatty acid with 18 carbon atoms of 5-30% by weight, (C) mono-, di-, tri- or penta-ester of polyglycerol with average polymerization degree of 3-6 and fatty acid with 18 carbon atoms of 1-18% by weight, and (D) water, wherein its average particle diameter is 110 nm or smaller. It is superior in acid resistance, salt-resistance and heat resistance, and further enables to maintain the good water-soluble state being blended to medicines, foods and beverages, cosmetics, feeds, additives usually employed therein.
CN102329246A Multiple-target-point tamibarotene derivatives, preparation method and purposes thereof The invention discloses multiple-target-point tamibarotene derivatives, a preparation method and purposes thereof. More specifically speaking, the invention provides a compound represented by a structural general formula (I), wherein the definition of R is referred to an instruction book; the derivatives are multiple-target-point compounds which are obtained by connecting tamibarotene as an RAR (retinoic acid receptors) excitant with various histone deacetylase inhibitors, various RXR (retinoid X receptors) excitants or other pharmacophoric groups directly through ester bonds or amido bonds or indirectly through connecting groups; and the derivatives are suitable to be used as antitumor drugs to be used for treating various malignant tumors, and are particularly suitable for treating various leukemia.
CN101244039A Novel method for preparing indissoluble medicaments liposome preparations The invention provides a new method for preparing an insoluble medicine lipidosome preparation, which is characterized in that the medicine can be carried on the dimolecular membrane via distributing and reducing grain diameter steps; and the preparation method is easy. The preparation method has the advantage of easily realizing the industrial production of the fat-soluble medicine lipidosome in virtue of the quite mature industrial production of the blank lipidsome at present.
US6906076 Inactivating a nuclear localization signal of a protein by contacting the protein with a compound that binds reversibly; parasiticides; viricides The present invention concerns alkyl aryl carbonyl compounds that possess anti-infective activity. The compounds of the invention can be used to target specific nuclear localization signal, thereby blocking importation of specific proteins or molecular complex into the nucleus of a cell. The invention encompasses methods of use of such compounds for treatment or prevention of infectious diseases, such as parasitic and viral diseases, including, for example, malaria and acquired immunodeficiency syndrome. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.
WO2009096579A1 Nutritional composition for prevention of hyperglycemia Disclosed is a nutritional composition for preventing hyperglycemia, which comprises a nitrogen source, a lipid and a sugar component, wherein the nitrogen source comprises free isoleucine and/or free leucine, the lipid comprises a middle-chain fatty acid triglyceride, and the sugar component comprises palatinose and/or trehalose. The nutritional composition has an excellent nutritional balance even when the nutritional composition is ingested for a long period, can prevent the development of hyperglycemia after the nutritional composition is administered, and enables the reduction in the amount of insulin to be administered.
WO2010136778A1 Dibenzothiophene derivatives as dna- pk inhibitors Compound formula I: wherein: X1 and X2 may be either (a) C and O, (b) N and N, or (c) C and NH, where the dotted bonds represents a double bond in the appropriate location; R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, or an optionally substituted C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; RN1 is selected from hydrogen and an optionally substituted C1-4 alkyl group; RC1 is selected from an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, or an optionally substituted C5-20 aryl group; or RN1 and RC1 may together form an optionally substituted C2-4 alkylene group.
CN101249153A Chinese and western drugs for curing bird bacillus coli disease and method of preparing the same The invention relates to a Chinese and western drug for treating avian escherichia coli diseases. The invention is characterized in that the Chinese and western drug comprises the components by weight parts as follows: rhubarb is 10 to 30 parts, radix scutellariae is 5 to 15 parts, coptis roots are 1 to 5 parts, radix isatidis is 1 to 5 parts, and enrofloxacin is 0.5 to 5 parts. The invention has a preparation method as follows: (1) the components are got by weight parts as follows: the rhubarb is 10 to 30 parts, the radix scutellariae is 5 to 15 parts, the radix isatidis is 1 to 5 parts, and the radix isatidis is 1 to 5 parts; (2) purified water which is 2 to 3 times the weight of the total quantity of all components is added, and concentrated solution is obtained after diacolation, evaporation and concentration, wherein, the relative density of the concentrated solution is 1.05 to 1.2; (3) the enrofloxacin which is 0.1 to 1 time the weight of the concentrated solution is added in the concentrated solution, and the purified water which is 2 to 5 the weight of the concentrated solution is added, so that the Chinese and western drug is made. The invention has strengthening efficacy after extraction and separation, effectively treats chicken escherichia infection, and reduces the economic loss of raising households. The Chinese and western drug realizes the reasonable collocation and combination by selecting various active ingredients, the cost is low, the curative effect is good, the cure rate is high, and the safety and the reliability are realized.
DE102005051862A1 Emulsion for treating e.g. skin aging comprises a lipid phase of polar and/or moderately polar, having specified interfacial tension toward water; and at least one 1,2-alkanediol having specified 1-octanol/water distribution coefficient An emulsion comprises (wt.%): a lipid phase (more than 40) of at least one lipid selected from polar and/or moderately polar, having an interfacial tension toward water of less than 30 mN/m; and at least one 1,2-alkanediol containing 4 - 8 carbon atoms, having 1-octanol/water distribution coefficient (Ig P-ow) of -1 - 3. An independent claim is included for a cosmetic preparation comprising the emulsion. - ACTIVITY : Dermatological. No biological data given. - MECHANISM OF ACTION : None given.
CN101797265A Application of belamcanda chinensis total isoflavone or isoflavone compounds in preparing medicaments and food for preventing and treating women's disease The invention relates to the technical field of medicaments, in particular to application of 12 isoflavone compound monomers comprising belamcanda chinensis total isoflavone or tecoridin, wild tectoridin, tectorigenin, iridin and the like in preparing medicaments and food for preventing and treating lower women's estrogen level and retarding womb and ovarian failure or climacteric syndrome. Animal experiment results show that the total isoflavone or 12 isoflavone compound monomers in the belamcanda chinensis have remarkable pharmacological effects of improving the estrogen level, promoting the growth of follicle, promoting epitheliosis of womb and vagina, retarding womb and ovarian failure, improving the expression of an epithelial cell estrogen receptor of the vagina and the like, so the total isoflavone or 12 isoflavone compound monomers can be used for preparing the medicaments or food for preventing and treating lower women's estrogen level and retarding womb and ovarian failure or climacteric syndrome. The application provides a new source for seeking a plant estrogen medicament.
EP1305047B1 Non-peptide ccr1 receptor antagonists in combination with cyclosporin a for the treatment of heart transplant rejection This invention is directed to pharmaceutical compositions useful in treating heart transplant rejection in mammals comprising a pharmaceutically acceptable excipient, a therapeutically effective amount of a non-peptide CCR1 receptor antagonist and a sub-nephrotoxic amount of cyclosporin A.
CN103565768A Repaglinide sustained release preparation and preparation method thereof The invention relates to a repaglinide sustained release preparation taken once a day and a preparation method thereof. The repaglinide sustained release preparation comprises oral administration unit dose of solid sustained release preparation (containing 3mg of repaglinide) for a beagle, average maximum blood concentration of the repaglinide sustained release preparation after being taken for 1.1-3.1 hours is 120-300ng/ml, and the repaglinide sustained release preparation has an obvious blood glucose reducing effect after being taken within 12 hours. The novel oral repaglinide sustained release preparation can realize sustained release of repaglinide, and stable blood concentration is obtained; time of the blood glucose reducing effect is prolonged, preparation taking frequency is reduced, and taking compliance of a patient is improved.
WO2010097243A3 Process for forming solid oral dosage forms of solifenacin and its pharmaceutically acceptable salts Pharmaceutical compositions comprising solifenacin or its pharmaceutically acceptable salts as the active pharmaceutical ingredient prepared by dry technological methods, preferably by the direct compression or roller compaction method, i.e. by the process in the absence of a liquid solvent, and the process for their preparation, are disclosed.
US6862890 Process for production of nanoparticles and microparticles by spray freezing into liquid The present invention provides a system and a method for the production of microparticles and nanoparticles of materials that can be dissolved. The system and method of the present invention provide quicker freezing times, which in turn produces a more uniform distribution of particle sizes, smaller particles, particles with increased porosity and a more intimate mixing of the particle components. The system and method of the present invention also produce particles with greater surface area than conventional methods. One form of the present invention provides a method for the preparation of particles. An effective ingredient is mixed with water, one or more solvents, or a combination thereof, and the resulting mixture is sprayed through an insulating nozzle located at or below the level of a cryogenic liquid. The spray generates frozen particles.
CN103755767A CDDO ethyl ester polymorphic substance and application thereof The invention relates to a polymorphism shape of a compound disclosed as Formula I (ethyl 2-cyano-3,12-dioxooleanane-1,9(11)diolefin-28-ester (CDDO ethyl ester)) and a method thereof for treating various diseases, such as cancers and inflammation accompanied by the cancers.
CN101851199B Substituted piperazine N-ethyl sulfonamide derivative and preparation and application thereof The invention provides a substituted piperazine N-ethyl sulfonamide derivative and medicinal salt thereof. The acyl chloride derivative thereof is obtained by chlorination of substituted sulfoacid by thionyl chloride; substituted L-type amino acid is reduced by lithium aluminium hydride reduction to obtain L-type alkamines compound; the L-type alkamines compound and the substituted sulfoacid derivative are carried out with coupling reaction and protected by mesyl chloride to obtain methanesulfonate derivative; mono-Boc protection piperazine is performed with substitution reaction and trifluoroacetic acid deprotection to obtain monosubstitution piperazine; and the monosubstitution piperazine is carried out with substitution reaction under the catalysis of organic amine to obtain the substituted piperazine N-Ethyl sulfonamide derivative. The virus activity test to five tumour cells in vitro by the compound provided by the invention shows that the in vitro virus activity test of the derivative shows the activity of parts of compound is higher than or comparative to positive control antitumor drug. The invention can be applied in preparing drug for preventing and curing tumour. The general formula of the compound of the invention is shown in the specification.
US20090143571 Novel genes and their use in the modulation of obesity, diabetes and energy imbalance The present invention relates generally to nucleic acid molecules encoding proteins associated with the modulation of obesity, diabetes and/or metabolic energy levels. More particularly, the present invention is directed to nucleic acid molecules and the recombinant and purified proteins encoded thereby and their use in therapeutic and diagnostic protocols for conditions such as obesity, diabetes and energy imbalance. The subject nucleic acid molecules and proteins and their derivatives, homologs, analogs, chemical equivalents and mimetics are proposed as therapeutic and diagnostic agents for obesity, diabetes and energy imbalance.
US20070043079 Heterocyclic compound containing nitrogen atom and use thereof The present invention relates to a medicament comprising the compound of formula (I) wherein all symbols have the same meanings as defined in the specification, a salt thereof or a prodrug thereof. The compound of the present invention is useful for the prevention and/or treatment of immune diseases such as various types of inflammation, autoimmune disease, allergic diseases, etc.; infection concerning inflammation or HIV infections (e.g. asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), organ transplantation rejection, immunosuppression, psoriasis, multiple sclerosis, optic neuritis, polymyalgia rheumatica syndrome, uveitis, vasculitis, human immunodeficiency virus infection (acquired immunodeficiency syndrome etc.), atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, osteoarthritis, ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacteria infection, diabetes, cancer metastasis, atherosclerosis, etc.).
EP1214925B1 Chemical peeling agent A chemical peeling agent containing the following components (A) and (B): (A) polyethylene glycol or other alcoholic compound as represented by the following general formula: B-[-(CH2CH2O)m(AO)n-H]a wherein B is an alcohol residue; AO is C3-18 alkylene oxide; a is 1 or above; m is 4 or above; and n is 0 or above, provided that m, number of ethylene oxide molecules added, must satisfy the requirement that the ethylene oxide chain moiety must account for at least 40 % of the molecular weight of the compound, and (B) a phenol compound, for example, salicylic acid, phenol or resorcin.
CN1569233A Method for manufacturing gene medicine for preventing and treating SARS and its medicinal prescription The invention integrates the RNA interference technology, human gene pool search technology, biological computer information technology, liposome technology and gene engineering technology. It provides a practical method to better design and prediction of high specific gene fragment for acquiring a highly effective gene medicine to deactivating a group of related pathopoiesia genes. The invention in particular relates to a method for choosing a pathopoiesia SARS target gene and determining isogenous siRNS or anti nucleotide sequence and other related auxiliary component to assemble the novel gene medicine for the prevention and treatment of the SARS virus infection. The invention concerns a prescription of gene medicine in further, in particular to a specific nucleotide containing, 21 pairs nucleotide constituting monochain or double chains oligonucleotide molecule.
CN101328199A SiRNA inhibiting human cell cycle protein A2 expression and use thereof The invention aims to provide siRNA for inhibiting human cyclin A2 and an application of the same. The target sequence corresponding to the siRNA is mRNA of the human cyclin A2; the length of the siRNA is between 16 and 30 bps; the siRNA contains the following nucleic acid sequences: 5'-CCA UUG GUC CCU CUU GAU UTT-3' and 5'-AAU CAA GAG GGA CCA AUG GTT-3' (SEQ ID NO:1); the 3' end of the siRNA has an extending structure containing 2 to 4 dT or 2 to 6 U; and the siRNA takes a hexamethylene diamine functional carbon nanotube as a carrier and makes the expression level of the mRNA of the human cyclin A2 of a K562 cell reduced by 60 to 95 percent through transfection. The siRNA is taken as an active ingredient and used for preparing an antineoplastic medicine for inhibiting cell proliferation and promoting apoptosis, and the content of the siRNA is between 0.001 and 99.999 percent.
US20100330023 Multifunctional Forms of Polyoxazoline Copolymers and Drug Compositions Comprising the Same The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
US7115648 use for treating type 2 diabetes, insulin resistance, syndrome X, hyperinsulinaemia, hyperglucagonaemia, cardiac ischaemia and obesity Heterocyclic amides of formula (1) wherein: R1 is independently selected from, for example, C1-6alkyl, C5-7cycloalkyl, C5-7cycloalkylC1-3alkyl, C1-6alkoxy, C5-7cycloalkoxy, C5-7cycloalkylC1-3alkoxy, heterocyclyl, heterocyclylC1-3alkyl, heterocyclyloxy or heterocyclylC1-3alkoxy, R2 is phenyl or heteroaryl; R3 is independently selected from hydrogen, halo, nitro, cyano, hydroxy, carboxy, carbamoyl, C1-4alkyl, C2-4alkenyl, C2-4alkyl, C1-4alkoxy, C1-4alkanoyl, fluoromethyl, difluoromethyl trifluoromethyl and trifluoromethoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
WO2010118025A1 Progesterone antagonists spiro condensed in position 17 with a difluoromethylene- substituted perhydrofurane group Described herein are compounds which exhibit progesterone antagonistic effects and methods of treating cancer using such compounds.
US20080108693 N-debenzoyl-N-tert-butoxycarbonyl-10-deacetyl taxol; antitumor activity; chemical stability New anhydrous crystalline form of docetaxel and process of making anhydrous docetaxel and docetaxel trihydrate are provided.
CN102813631A Method for preparing phentolamine mesilate freeze-drying powder injection The invention discloses a method for preparing a phentolamine mesilate freeze-drying powder injection. The method comprises steps of preparing phentolamine mesilate solution for injection and freeze-drying. An adopted freeze-drying curve is as follows: a) pre-freezing; b) sublimation drying; c) first resolution; d) pressure rising and moisture absorption; and e) second resolution. A special pressure rising and liquefying process is adopted during the preparation process, and a denser vitrification layer is formed on the surface of the obtained product, thereby strong moisture absorption of inside loose structure of the product can be prevented, moisture absorption of the product after being dried can be effectively avoided, the occurrence of shrunk products is further reduced, the percentof pass of the products is significantly improved, and the cost is reduced. The method for preparing the phentolamine mesilate freeze-drying powder injection has better economic benefits and social benefits.
WO2008063346A2 IL-14α RNA INHIBITORS AND ANTIBODIES TO IL-14α FOR TREATMENT OF AUTOIMMUNE DISEASES AND LYMPHOMAS Provided are antisense poly-2'-O-(2,4-dinitrophenyl) oligoribonucleotides which are complementary to the IL-14α gene and/or transcribed IL-14α mRNA. Also provided are monoclonal antibodies reactive with discreet IL-14α peptides. The oligoribonucleotides and monoclonal antibodies are useful in inhibiting the growth of lymphocytes.
CN103393625A Application of fungus polyketide in preparation of medicine used for treating alzheimer disease The invention relates to an application of fungus polyketide in preparation of a medicine used for treating alzheimer disease. According to the application, a fungus polyketide compound is prepared into an injection preparation used for treating the alzheimer disease, molecular weight of the fungus polyketide compound is 478.434Da, and 10mg/Kg injection preparation is intraperitoneally injected everytime; the fungus polyketide compound overcomes the defects that similar medicines in the past can not influence a pathological process and specificity can not be determined; a fungus polyketide compound injection medicine is adopted, is a small molecule compound, can penetrate through a blood brain barrier and can act on a pathological process of the alzheimer disease (AD), a decision for developing a medicine used for treating AD at present is met, an Abeta nerve toxic effect can be directly inhibited, and Abeta-induced nerve cell apoptosis is inhibited, namely nerve cell apoptosis is reduced by activating an Akt/GSK-3beta/beta-catenin signal channel.
WO2011115725A3 Indazole compounds as kinase activity modulators for the treatment of cancer and related disorders The present application relates to substituted 1 H-indazole compounds that are useful as kinase-activity modulators in the treatment of cancer and related diseases.
US7094809 Topical administration of dihydroxytoluene to block viral replication The present invention provides a method of inhibiting the formation of infectious herpes virus particles, particularly infectious herpes simplex virus (HSV) particles, in a host cell. The method involves administering an effective amount of a hydroxylated tolan, particularly a polyhydroxylated tolan, to a herpes virus infected host cell. The present invention also provides a method of treating a herpes virus infection, particularly an HSV infection. The method comprises administering a topical composition comprising a therapeutically effective amount of a hydroxylated tolan to a herpes virus-infected site. The present invention also relates to a topical composition for treating a herpes virus infection selected from the group consisting of an HSV infection, a cytomegalovirus infection, and a varicella zoster virus infection. The present invention also provides a method of treating a subject infected with Neisseria gonorrhea.
EP1697332A1 Benzo'1,4 ! diazepin-2-one derivatives as phosphodiesterase pde2 inhibitors, preparation and therapeutic use thereof The invention relates to compounds of formula (I) having PDE2 inhibitory activities, as well as therapeutic methods by administering said compounds, in particular for treating various diseases of the central or peripheral nervous system. It further deals with pharmaceutical compositions comprising said compounds and methods for preparing said compounds. Compounds of general formula (I).
US7371773 2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile; drug transporter, which actively transports an anticancer drug out of cancer cells, antagonist; improve drug resistance; anticarcinogenic agent; enhance bioavailability of anticancer drug The invention provides a drug which inhibits BCRP. A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH3 group); a cyano group (—CN group); a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2 (n=1−7: R2 is hydrogen or C1-C4 alkyl), —OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., —OP(O) (OH)2) or a salt thereof, a sulfate group (i.e., —OSO3H) or a salt thereof, a glycopyranosyl group or a salt thereof, a phosphate ester of a glycopyranosyl group or a salt of the ester, a sulfate ester of a glycopyranosyl group or a salt of the ester, or a piperidinopiperidinocarbonyloxy group], an ester thereof, or a salt thereof.
WO2014116121A1 Assembly of micelle aggregates of surfactant micelles and silver nanoparticles and use as antibacterial agent An assembly of micelle aggregates, wherein each aggregate comprises micelles of an anionic surfactant and nano-sized particles of metallic silver. A product comprising such assemblies for use in treating or preventing bacterial infections.
CN103202423A Fructus trichosanthis polysaccharide composite capsule and preparation method thereof The invention belongs to the technical field of a composite capsule, and particularly relates to the technical fields of a fructus trichosanthis polysaccharide composite capsule and a preparation method thereof. The fructus trichosanthis polysaccharide composite capsule comprises the materials of 10-30 parts of fructus trichosanthis polysaccharide, 10-30 compound powder of rhizoma anemarrhenae and dried rhizome of rehmannia, 2-10 parts of beta-cyclodextrin, 20-40 parts of starch and 15-25 parts of sodium alginate. The fructus trichosanthis polysaccharide composite capsule is developed from the fructus trichosanthis polysaccharide, rhizoma anemarrhenae and dried rhizome of rehmannia as main materials, and other auxiliary materials; the preparation process of the fructus trichosanthis polysaccharide composite capsule is carried out at normal temperature; the operation process is safe and convenient; and no water or gas which is harmful to the environment is generated in the preparation process. The polysaccharide composite capsule is easy to be absorbed by a human body, and convenient to carry, and can fully express the nutritive value and the medicinal value of the fructus trichosanthis, the dried rhizome of rehmannia and the rhizoma anemarrhenae.
CN103142533A Enteric coated tablet of etoposide The invention relates to an enteric coated tablet of etoposide. The etoposide is prepared into an inclusion compound, and then the inclusion compound is prepared into the enteric coated tablet.
US20060057254 Zinc-rich foods having effect of preventing diabetes Zinc (II) ions (zinc sulfate, zinc acetate and the like) originated in inorganic salts making it difficult for such ions to pass through biological membranes, thus being difficult to be incorporated in a human body. For overcoming such problems, it is necessary to develop food products with a prophylactic effect against diabetes, which contain zinc sources and have a lower toxicity than zinc (II) ions, a good stability and good fat-solubility. The present invention provides food products which have a prophylactic effect against diabetes using specified health foods, nutritional (functional) foods or the like containing natural substances that contain zinc in high concentrations (plants such as papaya, maca and the like, and yeasts such as baker's yeast, brewer's yeast and the like).
WO2014153090A1 Pyrazole derivatives asprmt1 inhibitors and uses thereof Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMTl activity. Methods of using the compounds for treating PRMTl - mediated disorders are also described.
US20090104178 Chemokine binding activity of viral tnf receptors and related proteins Chemokine binding activity of viral TNF receptors and related proteins. The invention relates to a C-terminal domain (CTD) of viral tumour necrosis factor receptors (vTNFRs) CrmB or CrmD or CTD homologues (CTD1, CTD2 and CTD3) from poxvirus and their functional homologues, including derivatives, and fragments, for use in binding chemokines and their analogues and/or to enhance the immunomodulatory properties of TNFRs or in bloking binding of chemokines to their corresponding cell surface receptors and/or to modulate chemokine biological activity.
WO2007070546A2 Meniscal implant of hyaluronic acid derivatives for treatment of meniscal defects A composite for treating an articular defect includes a hyaluronic acid derivative; and at least one member of the group consisting of a cell, a cellular growth factor and a cellular differentiation factor, which is impregnated in, or coupled to. the hyaluronic acid derivative. In one embodiment, carboxyl functionalities of the hyaluronic acid derivative are each independently derivatized to include an N-acylurea or O-acyl isourea, or both N-acylurea and O-acyl isourea. In another embodiment, the hyaluronic acid derivative is prepared by reacting an uncrosslinked hyaluronic acid with a biscarbodimide in the presence of a pH buffer in a range of between about 4 and about 8. The composite can be used for regenerating or stimulating regeneration of meniscal tissues in a subject in need thereof.
EP2522346A1 Agent combinations of Hesperidin for treating sleep disorders Active agent combination (I) comprises hesperidin or its salts and/or aglycone hesperetin, and at least one further active compound. An independent claim is included for sleeping pills or dietary supplements comprising (I). - ACTIVITY : Hypnotic; Anabolic. - MECHANISM OF ACTION : None given.
CN102008442A Preparation method of fluorocarbon vesicle medicament carrying preparation The invention relates to a preparation method of a fluorocarbon vesicle medicament carrying preparation. The method comprises the following specific steps of: (1) dissolving fluorocarbon in ethanol and fully stirring and mixing so as to obtain ethanol solution of the fluorocarbon; (2) dissolving a surfactant in water, adding a cosurfactant, heating to raise the temperature and oscillating ultrasonically at a certain temperature so as to promote the formation of vesicles; and (3) mixing a certain amount of ethanol solution of the fluorocarbon and solution of vesicles, fully stirring and mixing under the protection of nitrogen gas, standing, performing centrifugal separation and extracting supernatant so as to prepare the fluorocarbon vesicle medicament carrying preparation. The preparation method is simple, has high operability and can further meet the requirements of production and application. The fluorocarbon vesicle medicament carrying preparation prepared by the preparation method can be well applied to the aspects of oxygen-poor first aid medicaments and the like.
CN1919169A Penciclovir emulsifiable paste and its preparation The invention relates to a Penciclovir dispersible paste which comprises Penciclovir 0.5-2.0 wt%, emulsifying agent 1.0-10.0 wt%, methyl glycol 5.0-20.0 wt%, antiseptic agent 0.01-0.5 wt%, glyceryl monostearate 1.0-5.0 wt%, hexadecyl alcohol 5.0-15.0 wt%, dahurian angelica root pieces 5.0-15.0 wt%, liquid paraffin 5.0-15.0 wt%, and balancing water. The invention also discloses the process for preparing the dispersible paste.
WO2008095679A1 Use of bartonella quintana derived lipopolysaccharide for the treatment of autoimmune, autoinflammatory or infectious diseases The present invention relates to a novel antagonis of the Toll-like receptor 4 (TLR-4). More specifically, the present invention relates to a lipopolysaccharide (LPS) isolated from the bacterium Bartonella, and especially Bartonella quintana, as a novel antagonist of the Toll-like receptor 4 (TLR-4). Further, the present invention relates t the use of said natural antagonist for the treatment of an autoimmune or inflammatory disease in a mammal and specifically for the treatment of rheumatoid arthritis (RA). Furthermore, the present invention relates to pharmaceutical compositions comprising a lipopolysaccharide (LPS) isolated from the bacterium Bartonella and especially Bartonella quintana.
CN101100474A Fluoroquinolone compound containing phosphate ester group and its preparation method and use A fluoquinolone compound containing organic phosphate base, its preparation and use are disclosed. In the general formula I, 5-bit methyl is (S)-structure or (R)-structure or (R/S) structure. The process is carried out by taking 1-tert-butoxy-carbonyl-4-hydroxy-piperidine as origin, reacting to obtain organic phosphate compound, treating to obtain 4-hydroxy-piperidine benzyl alcohol organic phosphate, reacting, column chromatography treating, and catalyzing hydrogenating to obtain final Icompound. It can be used to prepare medicines in treatment of infectious diseases.
US7317006 Thieno[2,3-d]pyrimidines with combined LH and FSH agonistic activity The invention relates to thieno[2,3-d]pyrimidine derivatives according to general formula I, or a pharmaceutically acceptable salt thereof, wherein N(R1)R2 are joined in a (2-6C)heterocycloalkyl ring. The compounds of the invention have LH as well as FSH receptor activating activity and can be used in fertility regulating therapies.
CN103721248A Chitosan oral mucosa ulcer patch The invention relates to a chitosan oral mucosa ulcer patch. The chitosan oral mucosa ulcer patch possesses antibacterial effects; can be positioned at diseased regions steadily without moving; is capable of repairing wounds, diminishing inflammation and stopping bleeding, resisting bacteria and sterilizing, promoting skin tissue healing and repairing, clearing away heat and toxic materials, and astringing wounds and relieving pain; is dry and comfortable, and is capable of preventing adhesion; and can be used for treating swollen sore throat, mouth and tongue sore, and other mucosa ulcer caused by heat toxin. Chitosan is taken as the main ingredient of the chitosan oral mucosa ulcer patch. The chitosan oral mucosa ulcer patch is a pure biological agent, and is suitable for treatment of a plurality of oral mucosa ulcers.
US7276501 6-(4-substituted-anilino)pyrimidine derivatives, method for preparation thereof and antiviral pharmaceutical composition comprising the same The present invention relates to 6-(4-substituted-anilino)pyrimidine derivatives useful as an antiviral agent, and more particularly novel 6-(4-substituted-anilino)pyrimidine derivatives having an excellent inhibitory effect on replication of Hepatitis C virus; HCV), represented by the following formula I: in which R represents a C1-C4 straight or branched alkoxycarbonyl group, heterocycliccarbonyl group or carboxyalkyl group; and pharmaceutically acceptable salts thereof, a preparation method thereof, and an antiviral pharmaceutical composition comprising the compound as an effective ingredient. The 6-(4-substituted-anilino)pyrimidine derivatives according to the present invention have an excellent inhibitory effect on replication of Hepatitis C virus (HCV) and thus can be advantageously used as a therapeutic or prophylactic agent of hepatitis C.
US20110313044 Polymorphs of Suberoylanilide Hydroxamic Acid The present invention is directed to a novel form of suberoylanilide hydroxamic acid and the processes for its preparation.
CN103623025A External reversal powder formula for restoring yang and preparation method thereof The invention provides an external reversal powder formula for restoring yang. The external reversal powder formula is characterized by comprising the raw materials by weight: 1-15g of fennel, 1-25g of potassium nitrate, 1-35g of akebiaquinata, 1-45g of realgar, 1-55g of herba asari, 1-60g of rhizoma atractylodis and 1-5g of borneol. A preparation method of the external reversal powder comprises the following steps: removing impurities; cleaning; baking; grinding; sieving; evenly mixing; evenly mixing into powder; feeding in a paper bag or a bottle, so as to obtain the product. The external reversal powder formula for restoring yang has first-aid effects on endemic plague, the first aid of a serious injury and suspended animation, the first aid of a sudden death, yang-restoring first aid, viscera stagnation, apoplexia, cholera, vomiting and diarrhea and bewitched symptoms.
US6908904 Pharmaceutical preparation and method for treatment of diabetes A method for treatment of a diabetic condition, wherein a therapeutically effective amount of at least one isoform of sulfatide is administered to a patient, wherein said at least one isoform of sulfatide upon administration to the patient affects the sulfatide metabolism in such a way that it results in an increased amount of sulfatide. Also the use of at least one isoform of sulfatide for the production of a pharmaceutical preparation for treatment of a diabetic condition is disclosed. Said isoform is preferably an isoform with 8-24 carbon atoms in the fatty acid chain, more preferably 12, 14, 16 or 18 carbon atoms, and most preferably 16 carbon atoms.
WO2012066319A1 Apomorphine by pulmonary inhalation, oprionally in combination with l-dopa or a dopamine agonist for use in the treatment of parkinson According to the invention there is provided a method of treating and/or preventing the symptoms of Parkinson's disease comprising delivering apomorphine, optionally in combination with levodopa and/or a dopamine agonist that is not apomorphine, wherein apomorphine is administered by inhalation.
WO2008139241A1 Uses of north american ginseng fractions for treating leukemia The invention is directed to a method of treating hematological malignancies by administering to the subject ginseng fractions from North American ginseng (Panax quinquefolium). The present invention can be used to activate the proliferation of hemopoietic cells in a patient in need of treatment, or as a therapeutic targeted at conditions characterized by hematological malignancy, such as an abnormal proliferation of blood cells, lymphocytes, multiple myeloma, etc. The invention also includes a method of treating leukemia by activating the proliferation of natural killer (NK) cells and monocytes in the bone marrow and the spleen of the patient by administering at least one ginseng fraction selected from the group consisting of CVT-E002, PQ2, PQ223 and purified fractions from CVT-E002, PQ2 and PQ223. The present invention may be used to treat the hematological malignancy or as a supplement for patients undergoing chemotherapy or radiation therapy.
CN102488705A Skin mucous membrane disinfectant for killing virus The invention belongs to the field of medicinal disinfection, and particularly relates to a skin mucous membrane disinfectant for killing virus. The disinfectant provided by the invention comprises the following components: composite quaternary ammonium salt, ortho-phthalaldehyde, povidone iodine or other colorless iodine, a synergist, a surfactant, chlorine dioxide, ethanol, a chelating agent, a stabilizer, essence and a pH adjusting agent.
CN103271878A Ceftezole sodium agent and preparation method thereof The invention relates to a ceftezole sodium agent and preparation method thereof, especially relates to a ceftezole sodium injection for treating microbe infection, and preferably relates to a freeze-drying powder injection. The mezlocilin sodium for injection mainly comprises the following components: ceftezole, and accessory sorbitol and arginine. The solvent in the injection of the present invention is injection water; the excipient in the freeze-drying powder injection is sorbitol, and sodium hydroxide or hydrochloric acid is used for adjusting pH valve.
CN101298455A Cephalosporin derivate containing triazolo pyridazinium The invention belongs to the technical field of medicine, in particular relates to a cephalosporin ramification containing triazolo pyridazine iodonium, the salt acceptable in medicine thereof, an ester easily hydrolytic thereof, a hydrate thereof and a hydrate of the salt or ester thereof which are shown in a general formula (I), wherein, R[1], R[2], R[3], R[4] and X are defined in an instruction; moreover, the invention also relates a preparation method of the compounds, medicine composites containing the compounds as well as the applications of the compounds used in the medicines for curing and/or preventing infectious diseases.
US20080181969 polypropylene theromplastic polymer, 3-(3,5-di-tert-butyl-4-hydroxyphenyl)-propionic acid and diphenyl disulfide antioxidants, silver sulfate as antimicrobial agent; improvements in color of melt-processed thermoplastic polymer A polymer composite comprising a thermoplastic polymer compounded with a phenolic antioxidant, an organo-disulfide antioxidant, and a silver-based antimicrobial agent. The specified combination of antioxidant stabilizers is superior in inhibiting undesirable discoloration of thermoplastic polymers in the presence of compounded silver-based antimicrobial agents. A process of preparing such a composite, comprising compounding the phenolic antioxidant and organo-disulfide antioxidant with the thermoplastic polymer prior to compounding the silver-based antimicrobial agent with the thermoplastic polymer.
WO2007149395A3 2,5-substituted oxazole derivatives as protein kinase inhibitors for the treatment of cancer Compounds of Formula (I) wherein R1 is chosen from optionally substituted phenyl, optionally substituted furanyl, optionally substituted thienyl, optionally substituted pyridinyl, and optionally substituted quinolinyl; X is CR2; R2 is hydrogen; L is chosen from a covalent bond, -CH2, -CH=CH-, -CH2O-, -CH2NHC(O)-, and -C(O> and R3 is chosen from optionally substituted aryl and optionally substituted heteroaryl, and exhibiting ATP- utilizing enzyme inhibitory such as, protein kinases, are disclosed. Protein kinase regulated diseases include, for example, the following general disease classes : cancer, autoimmunological, metabolic, inflammatory, infection, diseases of the central nervous system, degenerative neural disease, allergy/asthma, angjogenesis, neovascularization, vasucolgenesis, cardiovascular, and the like.
US20120064092 Novel Target for Regulating Multiple Sclerosis Methods are provided for decreasing demyelinating inflammatory disease in a subject by inhibiting the activity of chemokine-like receptor 1 (CMKLR1). Methods are also provided for screening for agents that find use in treating demyelinating inflammatory disease in a subject.
EP1235812B1 Pyrimidine derivatives as selective inhibitors of cox-2 The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof, in which: R?1 and R2¿ are independently selected from H, C¿1-6?alkyl, C2-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl or C4-12bridged cycloalkane; and R?3¿ is C¿1-6?alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
US20070202101 Combination therapy using anti-EGFR antibodies and anti-hormonal agents The invention relates to a combination therapy for the treatment of tumors and tumor metastases, preferably breast and prostate tumors, comprising administration of anti-EGFR (Her1) antibodies and anti-hormonal agents, optionally together with cytotoxic/chemotherapeutic agent. The method and the pharmaceutical compositions comprising said agents can result in a synergistic potentiation of the tumor cell proliferation inhibition effect of each individual therapeutic agent, yielding more effective treatment than found by administering an individual component alone.
US7994188 Compounds for treating inflammatory diseases The invention relates to the use of (1α.2β,4β.5α.7β)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane salts for preparing a pharmaceutical composition for the prevention and treatment of diseases associated with inflammation.
CN102850328A Pyridine chemical, its preparation method, and pharmaceutical composition containing the chemical and application thereof The invention relates to a pyridine chemical shown as the following general formula and having c-Met and/or ALK inhibitory activity and its pharmaceutically-acceptable salt or pharmaceutically-acceptable solvate, a preparation method thereof, a pharmaceutical composition containing the chemicals, and applications of the chemicals in preparation of medicines for preventing and treating abnormal proliferation and morphological change of cells and related diseases, such as hyperkiesis, related to hepatocyte growth factor receptor (HGFR) and/or anaplastic lymphoma kinase (ALK) in organism and diseases related to vascularization or cancerometastasis, especially application in preparation of medicines for treating and preventing growth and metastasis of tumor.
CN101152157A Meloxicam orally disintegrating tablets and method for preparing the same The invention discloses a meloxicam orally disintegrating tablet, which is of reasonable formula and good vioavailability, and the preparation method. The content of the principal agent of the meloxicam orally disintegrating tablet, meloxicam, is 5 to 20 percent. The excipient contains disintegrant, diluent or binder, adhesive, sweetener, arom atic agent, lubricant, etc. The preparation method adopts modern preparation technology and the product has stable quality. So the preparation method provides patients with safe and effective meloxicam orally disintegrating tablet.
EP2781525A2 Novel derivatives of hemin with antibacterial and antiviral activity The invention relates to novel hemin derivatives of general formula (I), preparing and use thereof as antibacterial and/or antiviral agents, including, as a component in a pharmaceutical compositions. Advantages of the novel antibacterial and antiviral agents based on the hemin derivatives are in their biocompatibility, biodegradability, a high efficacy against resistant bacteria and widespread viruses which are dangerous to humans, and the lack of toxicity.
CN102976975A Aryl propionyl-N-methyl hydroxamic acid urease inhibitor, synthesis and application thereof The invention discloses aryl propionyl-N-methyl hydroxamic acid compounds, which have the following structural general formula: FORMULA (referring to the specification). The aryl propionyl-N-methyl hydroxamic acid compounds have good inhibition action to urease and can be used for preparing medicines for resisting gastritis, gastric ulcer and lithangiuria. The invention discloses the preparation methods of the aryl propionyl-N-methyl hydroxamic acid compounds.
US20120225872 Methods of preparing and using quinazoline and quinoline derivatives A method of preparing a compound of formula (I), A method for treating cancer or inhibiting growth of cancer cells including administering to a patient mammal in need thereof a pharmaceutical preparation including the compound. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal including administering to a mammal a pharmaceutical preparation including the compound.
US20110071223 Body cosmetics for wetted skin A body cosmetic for application to wetted skin after bathing, and the like, which provide high moisturizing effects, spread well to all over the body, and are easy to apply. An oil-in-water body cosmetic for application to wetted skin, which contains a water-soluble polymer and the following components (A) to (C): (A) from 20 to 50% by mass of oily ingredients containing (A1) oil that is pasty at 25° C. and (A2) polar oil that is liquid at 25° C.; (B) from 11 to 50% by mass of glycerin; and (C) from 20 to 60% by mass of water; in this body cosmetic for application to wetted skin, the content of the pasty oil (A1) is from 1 to 20% by mass, and the content of the liquid polar oil (A2) is from 1 to 20% by mass.
US20080051360 Pkc ligands and polynucleotides encoding pkc ligands The invention relates to kinase ligands and polyligands. In particular, the invention relates to ligands, homopolyligands, and heteropolyligands that modulate PKC activity. The ligands and polyligands are utilized as research tools or as therapeutics. The invention includes linkage of the ligands, homopolyligands, and heteropolyligands to a cellular localization signal, epitope tag and/or a reporter. The invention also includes polynucleotides encoding the ligands and polyligands.
WO2010085820A2 Tricyclic compounds as antagonists of prostaglandin d2 receptors Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
CN102895464A Medicament for treating children diarrhea The invention discloses a medicament for treating children diarrhea. The medicament is prepared by the following steps of: mixing medicaments including scorched large-head atractylodes rhizome, officinal magnolia bark, dried orange peel, indian buead, oriental waterplantain rhizome, scorched medicated leaven, scorched fructus crataegi, chicken gizzard membrane, dark plum fruit, Chinese yam, umbellate pore fungus, red halloysite and roasted liquoric root uniformly in parts by weight; adding water for decocting for 2-4 times, every time for 1-2 hours; combining decoctions; filtering; concentrating a filtrate into clear paste of which the relative density is 1.15-1.18 at the temperature of 70 DEG C; refrigerating and standing; filtering a supernatant; adding conventional auxiliary materials into the filtrate; mixing uniformly; adding purified water till the medicament content is 1g/mL; and filling and sterilizing to obtain an oral liquid preparation. The medicament disclosed by the invention has the effects of depressing qi, relieving flatulence, strengthening the spleen, replenishing qi, promoting the circulation of qi, dissipating blood stasis, dissolving turbidity, lowering lipid, regulating qi-flowing for strengthening spleen and promoting digestion, and has a remarkable curative effect on children diarrhea.
WO2011053511A1 Heteroaryl substituted arylindenopyrimidines and their use as highly selective adenosine a2a receptor antagonists This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. Formula (I) wherein X, R2, R3, and R4 are as defined in the specification.
WO2013111850A1 Chromone derivative having osteogenesis promoting effect The present invention addresses the problem of providing a compound or a pharmacologically acceptable salt thereof, said compound being to be used for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture and preventing or treating diseases relating to bone metabolism, or for promoting healing in bone diseases such as bone fracture, bone defect or osteoarthritis in the field of plastic surgery and treating periodontal disease or stabilizing artificial tooth roots in the field of dentistry. Provided is a compound represented by general formula (I) or a pharmacologically acceptable salt thereof. The meanings of the substituents in formula (I) are as follows: R1 represents a halogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 represents a hydrogen atom, etc.; and A represents a heterocyclic group, etc.
US20080044364 Flavonoid Complexes The invention relates to compounds of the formula I where R1 to R10 may be identical or different and are selected from H, OR11, straight-chain or branched C1- to C20-alkyl groups or hydroxyalkyl groups, straight-chain or branched C3- to C20-alkenyl groups and/or C3- to C12-cycloalkenyl groups, where the rings may each also be bridged by —(CH2)n— groups, where n=1 to 3, where all OR11, independently of one another, stand for OH, C1- to C20-alkoxy groups, C3- to C20-alkenyloxy groups, straight-chain or branched C1- to C20-hydroxyalkoxy groups and/or C3- to C10-cycloalkoxy groups and/or C3- to C12-cycloalkenyloxy groups, where the rings may each also be bridged by —(CH2)n— groups, where n=1 to 3, and/or mono- and/or oligoglycosyl radicals, CD stands for a cyclodextrin molecule, o stands for the number 1 and p stands for a number from the range 0.5 to 50, with the proviso that at least 2 radicals from R1 to R7 stand for OH and that at least 1 pair of adjacent —OH groups is present in the molecule.
CN103012540A 22-drop-6-hydroxystigmast-3,22-O-dimethyloxime ether and 22-drop-6-oximido-stigmast-3,22-O-dimethyloxime ether and application thereof to preparation of antitumor drugs The invention discloses 22-drop-6-hydroxystigmast-3,22-O-dimethyloxime ether and 22-drop-6-oximido-stigmast-3,22-O-dimethyloxime ether which have the chemical structure formulas described in the specification. Experiments prove that the 22-drop-6-hydroxystigmast-3,22-O-dimethyloxime ether and the 22-drop-6-oximido-stigmast-3,22-O-dimethyloxime ether have remarkable inhibition functions to various tumor cell strains, and can be applied to the preparation of drugs for treating various kinds of cancers.
CA2564207A1 Novel substituted thiophenecarboxamides, their production and their use as medicaments The invention relates to novel substituted thiophene-2-carboxamides of general formula (I), in which A, and R1 to R8c are defined as cited in claim 1. The invention also relates to the tautomers, enantiomers, diastereomers, mixtures and salts, in particular the physiologically compatible salts of said compounds containing inorganic or organic acids or bases, which exhibit valuable properties.
US20110207813 Pharmaceutical composition with gelling properties containing a tyrosine derivative The present invention relates to an injectable pharmaceutical composition with gelling properties containing:—an active principle; a hydrophobic and bio-compatible organic liquid; and an organogelling substance, the molecules of which have the capacity to bind together via bonds of low energy, wherein said organogelling substance is chosen among L-tyrosine derivatives responding to the following formula (I) wherein: R1 is an alkyl group containing 1 to 3 carbon atoms, linear or branched; and R2 is a hydrophobic group chosen among aliphatic saturated or unsaturated fatty chains or aryl or arylalkyl groups, Its use as a vector for the release of active principles, as well as its process of preparation.
CN101156847B Usage of purplish plastocyanin as insulin sensitization agent The invention discloses the usage and the formulation of Zilanine used as insulin sensitizing agent, in particular, the usage of the Zilanine of the invention is an application in preparing the insulin sensitizing agent which can improve pathological change of liver, and the application in preparing the insulin sensitizing agent which can improve pathological change of kidney; the formulation of the Zilanine used as the insulin sensitizing agent of the invention is the insulin sensitizing agent which can improve the pathological change of the liver and is prepared with the Zilanine as an effective ingredient, and the insulin sensitizing agent which can improve the pathological change of the kidney and can be prepared with the Zilanine as the effective ingredient.
EP1531869A2 Compositions and methods for treating cancer using maytansinoid cd44 antibody immunoconjugates and chemotherapeutic agents The invention relates to the combined use of conjugates of CD44 specific antibodies with cytotoxic compounds and chemotherapeutic agents in cancer therapy, pharmaceutical compositions comprising such compounds and/or chemotherapeutic agents, and methods of cancer treatment. Preferred conjugates contain maytansinoids as cytotoxic compounds, and preferred chemotherapeutic agents are taxanes.
CN101798303B Azole derivatives, preparation method and application thereof The invention belongs to the technical field of antifungal medicaments, and provides azole derivatives with a structure of a general formula (I) and pharmaceutically acceptable salts thereof, wherein definitions of A, B, Y and R are as described in instructions. The invention also relates to a preparation method for the compounds, and also discloses medicinal compositions taking the compounds andthe pharmaceutically acceptable salts thereof as active ingredients, as well as application thereof in the aspect of acting as antifungal medicaments.
US20130012494 Cyclopropyl-fused-1,3-thiazepines as bace1 and/or bace2 inhibitors The present invention provides cyclopropyl-fused-1,3-thiazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
WO2014099696A1 2-pyridyloxy-4-ester orexin receptor antagonists The present invention is directed to 2-pyridyloxy-4-ester compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ester compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
US20090203634 Compositions and Uses of Amooranin Compounds Amooranin (AMR) has been found to cause tumor cell death through G2/M cell cycle arrest, caspase activation, and apoptosis. Furthermore, it has been demonstrated that AMR is a substrate for P-glycoprotein. Based on these activities, AMR compounds, including AMR analogs, can be used in the treatment of a number of diseases in which aberrant cellular proliferation occurs such as drug-sensitive and drug-resistant cancers, autoimmune disorders, and inflammatory diseases.
CN101684094A 3-substituted-1, 8-naphthalimide compound and synthesis method and medical application thereof The invention relates to a 3-substituted-1, 8-naphthalimide compound with a structural general formula shown on the right in and a synthesis method and a medical application thereof. The pharmacological test proves that the 3-substituted-1, 8-naphthalimide compound of the invention has good effect for inhibiting the growth of tumor cells.
WO2014138812A1 Salts, co-crystals, and polymorphs of an anxiolytic compound The present invention provides amorphous arid crystalline forms of 1-ethyl-6-(indan-2- ylamino)-3-(morpholine-4-carbonyl)-1,8-naphthyridin-4-one (compound 1), and salts, co- crystals, and pharmaceutical compositions thereof. The invention also provides methods of treating and/or preventing a disease, such as a central nervous system disease (e.g., an anxiety disorder), using the amorphous and crystelline forms, and salts, co-crystals, and pharmaceutical compositions thereof.
US20070254871 Compounds for the Treatment of Inflammation of the Central Nervous System KATP channel openers (KCOs) are useful for the prophylactic and/or therapeutic treatment of CNS chronic inflammation associated with a disease or state in a mammal, including a human. The administration of KCOs, including the groups of benzopirans, cyanoguanidines, thioformamides, benzothiadiazines, pyridyl nitrates, pyrimidine sulfates, cyclobutenediones, DHP-related compounds, tertiary carbinols, 6-sulfonil-chromenes, 1,2,3-triazoles, pyridothiadiazines, benzothiazines, halogenquinazolins and phenylbenzimidazoles, and in particular, the compound diazoxide, result in a reduction of reactive microglial response in various CNS pathologies such as axonal injury, brain tumors, traumatic damage, neurodegeneration, spinal cord injury, infectious and autoimmune diseases. KCOs, isotopically modified, are also useful for the preparation of diagnostic agents for detection and follow-up of CNS chronic inflammation.
US20080242701 Antitumor agents; anticancer agents; cytotoxic activity; angiogenesis inhibitor; leukemia; colorectal cancer; administering by mouth This invention relates to treating cancer or an angiogenesis-related disease using a compound of formula 1: wherein R1, R2, R3, R4, and n are defined herein.
CN102702215A Compound mangostenone F, preparation method and application in preparation of antitumor drugs thereof The invention discloses a compound mangostenone F, a preparation method and application in preparation of antitumor drugs thereof. The novel compound mangostenone F disclosed by the invention is separated from mangosteens and purified. The compound mangostenone F shows an obvious cytotoxic activity against nasopharyngeal carcinoma CNE-1 cell lines, nasopharyngeal carcinoma CNE-2 cell lines, lung cancer A549 cell lines, lung cancer H460 cell lines, gastric cancer SGC-7901 cell lines, prostate cancer PC-3 cell lines and human glioma U87 cell lines and inhibition effect is obvious. The compound mangostenone F can be used to prepare the antitumor drugs. The invention provides a lead compound for researching new antitumor drugs and has an important significance for developing fruit medical biological resources.
EP1562560A1 Modified release composition comprising a short-acting hypnotic for treatment of sleep disorders A pharmaceutical composition comprising a first component comprising a short-acting hypnotic or a pharmaceutically acceptable salt thereof; a second component comprising at least one particle, wherein the at least one particle comprises a core and at least one coating over the core, the core comprising a short-acting hypnotic or a pharmaceutically acceptable salt thereof, and the at least one coating comprising at least one pharmaceutically acceptable polymer that is soluble at a pH greater than or equal to about 5.5, and optionally a third component comprising at least one particle, wherein the at least one particle comprises a core and at least one coating over the core, the core comprising a short-acting hypnotic or a pharmaceutically acceptable salt thereof, and the at least one coating comprising at least one pharmaceutically acceptable polymer that is soluble at a pH greater than or equal to about 6.0. Methods of treating sleep disorders, prolonging sleep, and inducing sleep using these compositions are also disclosed.
EP1216247B1 Imidazoimidazoles and triazoles as anti-inflammatory agents Compounds of formula (I) which are useful for treating or preventing inflammatory and immune cell-mediated diseases.
US20110213011 Modulation of smad3 expression Provided are compounds capable of inhibiting SMAD3 and compositions containing same as well as methods using such compounds for treating fibrosis and scarring.
DE102008057364A1 New pyridyl or phenyl ring containing compounds are hypoxia-inducible factor regulation pathway modulators, useful to treat and/or prevent e.g. cancer or tumor diseases, heart attack, arrhythmia, stroke, psoriasis and diabetic retinopathy Pyridyl or phenyl ring containing compounds (I) and their solvates, salts or solvate of the salts are new. Pyridyl or phenyl ring containing compounds of formula (I) and their solvates, salts or solvate of the salts are new. Ring A : pyridyl or phenyl ring; ring B : 1H-pyrazole group of formula (a1) or (b1), 1H-imidazole group of formula (c1), 1H-pyrrole group of formula (d1), or 2H-pyrrole group of formula (e1); a : connection point with the adjacent CH 2-group; aa : connection point with the ring (D); ring D : [1,2,4]oxadiazole group of formula (f1) or (g1), [1,3,4]oxadiazole group of formula (h1), oxazole group of formula (i1)-(l1), isoxazole group of formula (m1) or (n1), or 1H-imidazole group of formula (o1); aaa : connection point with the ring B; aaaa : connection point with the ring (E); ring E : phenyl or pyridyl ring; R 1>H, halo, CN, (1-6C)-alkyl, (2-6C)-alkenyl, (2-6C)-alkynyl, (3-6C)-cycloalkyl, -OR 6>, -SR 6>, -S(=O)-R 6>, -S(=O) 2-R 6>, -C(=O)-OR 6>, -C(=O)-NR 6>R 7>, -S(=O) 2-NR 6>R 7>, -NR 6>R 8>, -N(R 6>)-C(=O)-R 7> or -N(R 6>)-S(=O) 2-R 7>, where (1-6C)-alkyl, (2-6C)-alkenyl or (2-6C)-alkynyl is optionally 2-3 times substituted by F, OH, (1-4C)-alkoxy, CF 3O, tri-(1-4C)-alkylsilyl, (1-4C)-alkoxycarbonyl or (3-6C)-cycloalkyl, and the cycloalkyl is optionally 2-3 times substituted by F, (1-4C)-alkyl, CF 3, OH, (1-4C)-alkoxy, CF 3O or (1-4C)-alkoxycarbonyl; R 6>, R 7>H, (1-6C)-alkyl or (3-6C)-cycloalkyl, where the (1-6C)-alkyl is optionally 2-3 times substituted by F, OH, (1-4C)-alkoxy, CF 3O, (1-4C)-alkoxycarbonyl or (3-6C)-cycloalkyl, the cycloalkyl is optionally 2-3 times substituted by F, (1-4C)-alkyl, CF 3, OH, (1-4C)-alkoxy, CF 3O or (1-4C)-alkoxycarbonyl; R 8>H, (1-6C)-alkyl, (3-6C)-cycloalkyl or 5- or 6-membered heteroaryl, where (1-6C)-alkyl is optionally 2-3 times substituted by F, OH, (1-4C)-alkoxy, CF 3O, (1-4C)-alkoxycarbonyl, (3-6C)-cycloalkyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl or 5- or 6-membered heteroaryl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl and cycloalkyl group is optionally 2-3 times substituted by F, (1-4C)-alkyl, CF 3, OH, (1-4C)-alkoxy or (1-4C)-alkoxycarbonyl, and the heteroaryl is 2-3 times substituted by F, Cl, CN, (1-4C)-alkyl, CF 3, (1-4C)-alkoxy or CF 3O; R 2>H, F, Cl, CN, CH 3, CF 3, OH, CH 3O or CF 3O; R 3>CH 3, C 2H 4 or CF 3; R 4>H, halo, CN, pentafluorothio, (1-6C)-alkyl, tri-(1-4C)-alkylsilyl, -OR 9>, -NR 9>R 1> 0>, -N(R 9>)-C(=O)-R 1> 0>, -N(R 9>)-C(=O)-OR 1> 0>, -N(R 9>)-S(=O) 2-R 1> 0>, -C(=O)-OR 9>, -C(=O)-NR 9>R 1> 0>, -SR 9>, -S(=O)-R 9>, -S(=O) 2-R 9>, -S(=O) 2-NR 9>R 1> 0>, (3-6C)-cycloalkyl, 4-6-membered heterocycle or 5- or 6-membered heteroaryl, where (1-6C)-alkyl for is optionally 2-3 times substituted by F, -OR 9>, -NR 9>R 1> 0>, -N(R 9>)-C(=O)-R 1> 0>, -N(R 9>)-C(=O)-OR 1> 0>, -C(=O)-OR 9>, -C(=O)-NR 9>R 1> 0>, (3-6C)-cycloalkyl, 4-6-membered heterocycle or 5- or 6-membered heteroaryl, the cycloalkyl- and heterocycle are 2-3 times substituted by F, (1-4C)-alkyl, CF 3, OH, (1-4C)-alkoxy, CF 3O, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, (1-4C)-alkylcarbonylamino, (1-4C)-alkoxycarbonylamino, (1-4C)-alkylcarbonyl or (1-4C)-alkoxycarbonyl, and the heteroaryl is optionally 2-3 times substituted by F, Cl, CN, (1-4C)-alkyl, CF 3, (1-4C)-alkoxy or CF 3O; either R 9>, R 1> 0>H, (1-6C)-alkyl, (3-6C)-cycloalkyl or 4-6-membered heterocycle, where the (1-6C)-alkyl is 2-3 times substituted F, OH, (1-4C)-alkoxy, CF 3O, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, (1-4C)-alkoxycarbonyl, (3-6C)-cycloalkyl or 4-6-membered heterocycle, and the cycloalkyl and heterocycle are optionally 2-3 times substituted by F, (1-4C)-alkyl, CF 3, OH, (1-4C)-alkoxy, CF 3O, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, (1-4C)-alkylcarbonyl or (1-4C)-alkoxycarbonyl; or R 9>R 1> 0>N : a 4-6-membered heterocycle further containing a heteroatom of N, O, S or S(O) 2 and 2-3 times substituted by F, (1-4C)-alkyl, CF 3, OH, (1-4C)-alkoxy, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, (1-4C)-alkylcarbonyl or (1-4C)-alkoxycarbonyl; R 5>F, Cl, CN, CH 3, CF 3 or OH; and n : 0-2. An independent claim is included for a medicament comprising (I) in combination with one or more inert, non-toxic auxiliary agent. - ACTIVITY : Cytostatic; Cardiant; Vasotropic; Antiarrhythmic; Cerebroprotective; Antipsoriatic; Ophthalmological; Antiinflammatory; Antiarthritic; Antirheumatic; Hemostatic; Vulnerary. - MECHANISM OF ACTION : Hypoxia-inducible factor regulation pathway modulator. The ability of (I) to modulate hypoxia-inducible factor regulation pathway was tested in HCT 116 cells using hypoxia-inducible factor luciferase assay. The results showed that N-methyl-5-[(5-methyl-3-{3-[4-(trifluoromethoxy)p henyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)methyl]pyridin-2-amine exhibited an IC 50 value of 2 nmole/l.
WO2012168885A3 Bisacodyl and its analogues as drugs for use in the treatment of cancer The present invention provides compounds having the formula A: (A) or pharmaceutically acceptable salt thereof, wherein W, R1, R2 and R5 are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as cytotoxic agents towards proliferating and/or quiescent cancer stem cells, and thus are useful, for example, for the treatment of cancer.
WO2012011407A1 Therapeutic agent for disease accompanied by epileptic waves Provided is a therapeutic agent for disease accompanied by epileptic waves that is easy to handle, has few side effects, and is immediate-acting. By controlling the carbon dioxide concentration of inhaled air, it is possible to alter the pH of body fluids to the acidic side and alleviate epileptic waves. Carbon dioxide is the active ingredient of the therapeutic agent for disease accompanied by epileptic waves.
CN1927168A Implantation slow release medicine in eyes The invention discloses an eye-implant sustained-release drug, which contains FK-506 macrolide antibiotics, absorbefacient /protectant and self-biodegradable drug carrier, the weight ratio of which is 1:0.05-1.5 : 0.25-4. The absorption enhancer / protectant is chitin polyose compounds, the chemical name of which is the poly-1, 4-beta-glucosamine and its chemical formula is (C6H11O4N)n, where n is 10-20. The absorption enhancer / protectant chitin polyose hydrochlorate, chitin polyose glutamate can greatly lower the transmembrane electric impedance of monomolecular membrane so as to increase its permeability and promote drug absorption. The drug releasing system of the invention releases drug under the interaction of the three, the drug can penetrate ocular barrier, achieve an effective ophthalmic drug concentration and strength and can be natural degraded in vivo physiological conditions, and thereby be absorbed, metabolised and excreted, it will not become the foreign body and not be a stimulus for the body or not produce foreign body reaction, so there is no need of second surgery to removed it.
CA2259460C Recombinant canine adenovirus (cav) containing exogenous dna Disclosed and claimed are recombinant adenoviruses, methods of making them, uses for them (including in immunological, immunogenic, vaccine or therapeutic compositions, or, as a vector for cloning, replicating or expressing DNA and methods of using the compositions and vector), expression products from them, and uses for the expression products. More particularly, disclosed and claimed are recombinant canine adenoviruses (CAV) and methods of making them, uses for them, expression products from them, and uses for the expression products, including recombinant CAV2 viruses. Additionally, disclosed and claimed are truncated promoters, expression cassettes containing the promoters, and recombinant viruses and plasmids containing the promoters or expression cassettes.
US20080311100 Treatment of Keratinous Dryness With Glycerides The present invention provides the use of medium chain glyceride(s) as an active ingredient for the preparation of a composition for oral and/or parenteral absorption and intended to prevent and/or treat dry and/or delicate keratinous substances.
US20080312164 Isothiocyanates and glucosinolate compounds and anti-tumor compositions containing same The present invention provides glucosinolate and isothiocyante compounds and related methods for synthesizing these compounds and analogs. In certain embodiments, these glucosinolate and isothiocyanate compounds are useful and chemopreventive and or chemotherapeutic agents.
CN102198127A Application of gambogic acid in preparing inflammation inhibitor The invention relates to an application of gambogic acid in preparing an inflammation inhibitor, in particular to an application of the gambogic acid in preparing medicaments for treating inflammatory factor mediated inflammatory diseases such as endotoxin shock and the like. The gambogic acid has a chemical formula of C38H44O8 and a molecular weight of 628.75, and can be used for preparing the medicaments for treating the inflammatory factor mediated inflammatory diseases such as endotoxin shock and the like, wherein the inflammatory diseases comprise rheumatic arthritis, inflammatory bowel disease, neurodegenerative disease, septic shock and the like. Approved by pharmacological experiments, the gambogic acid can effectively inhibit inflammatory factors such as tumor necrosis factor (TNFalpha), interleukin 6 (IL-6) and nitric oxide (NO), and can be used as an inflammation inhibitor for preparing the medicaments for treating the inflammatory factor mediated inflammatory diseases such as rheumatic arthritis, inflammatory bowel disease, neurodegenerative disease, septic shock and the like.
CN103446148A Application of Lycojaponicumin C in anti-influenza A virus drug The invention discloses application of Lycojaponicumin C in preparation of an anti-influenza A virus drug. An experiment proves that the Lycojaponicumin C has remarkable inhabiting effect on influenza A virus fluA and has potential application value in the field of treatment of influenza A virus infectious diseases. The application of the Lycojaponicumin C in the preparation of the anti-influenza A virus drug is disclosed for the first time. Due to the fact that the skeleton type is a novel skeleton type and the high influenza virus inhibiting activity of the Lycojaponicumin C is previously unimagined, the possibility that other compounds give any revelation does not exist, and the Lycojaponicumin C has outstanding substantive characteristics and meanwhile has a remarkable improvement in prevention and treatment of influenza virus infection obviously.
CN101919960A Inflammation and heat clearing tablets and preparation method thereof The invention discloses inflammation and heat clearing tablets. 1,000 inflammation and heat clearing tablets are prepared from raw materials of 160 to 180g of inflammation and heat clearing extract powder, 150 to 170g of filler, 13 to 15g of disintegrating agent, 0.8 to 2.0g of lubricating agent, 10 to 20g of silicon dioxide, 1.5 to 3.5g of menthol, 136 to 138g of baical skullcap root, a proper amount of povidone and a proper amount of ethanol by wet-process granulation and tabletting, wherein the inflammation and heat clearing extract powder is prepared by spray drying of inflammation and heat clearing extract. The invention also discloses a method for preparing the inflammation and heat clearing tablets. The tablets prepared by dissolving the menthol and the proper amount of ethanol, adding the silicon dioxide, mixing with the dry extract powder and tabletting have the stability effectively improved, and solve the problems of unqualified menthol identification, non-uniform content and unqualified hardness so as to improve product quality; and the method has the advantages of simple process flow, energy conservation, cost conservation and suitability for industrial production.
WO2008070995A1 Methods and treatments for prevention of acute renal failure following cardiac surgery Methods and treatments of prevention of, or reduction of risk of incidence of, acute renal failure following cardiac surgery, through administration of pyridoxal-5'-phosphate, pyridoxine, pyridoxal, pyridoxamine or a pyridoxal analogue, before, during or after the surgery. Of particular interest is when the cardiac surgery is Coronary Artery Bypass Grafting (CABG)
EP2246051A1 Method for production of orally rapidly disintegrating tablet comprising imidafenacin as active ingredient The present invention herein provides an imidafenacin-containing orally rapidly disintegrating tablet which is excellent in the photostability. The present invention comprises the steps of: (A) granulating imidafenacin together with starch to thus give a granulated product having an imidafenacin concentration ranging from 0.001 to 3% by mass and a starch concentration ranging from 40 to 99.999% by mass; (B) covering the granulated product prepared in the step (A) with a non-cellulosic coating agent; and (C) blending the granulated product obtained in the preceding step (B) with an excipient and a disintegrating agent and then forming the resulting mixture into a tablet according to the compression molding technique.
WO2008112498A2 Synthesis and characterization of polymorph form ii of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile A polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form II are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. Further provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.
CN101433518A Compound ofloxacin injection for animals The invention discloses compound ofloxacin injection for livestock, and belongs to medicine preparation containing organic effective components, or anti-infective medicament for the livestock. The injection of each 1, 000 liters is prepared by the following raw materials: 100 to 400 kilograms of sodium salicylate, 5 to 110 kilograms of ofloxacin, 10 to 150 kilograms of mequindox, 1 to 20 kilograms of atropine sulfate, 1 to 20 kilograms of dexamethasone sodium phosphate, and the balance being water for injection. The injection adopts combination of medicaments such as the ofloxacin, the atropine sulfate, the mequindox, and the like, can enhance curative effect, treats both symptoms and root causes, can effectively relieve stress reaction of sick livestock body, can be widely applied to treating pig scour, improve livability of pigs, and increase weight of the pigs.
EP2571354A1 Methods for inhibiting muscle atrophy In one aspect, the invention relates methods for inhibiting or preventing muscle atrophy or increasing muscle mass by providing to a subject in need thereof an effective amount of ursolic acid, a derivative thereof, or an analog of the ursane scaffold. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
CA2138287C N-substituted azabicycloheptane derivatives, the preparation and use thereof Compounds of the formula I:(See formula I) in which the substituents have the meanings stated in the description, and their preparation are described. These novel compounds are suitable as neuroleptics, antidepressants, sedatives, hypnotics, CNS protectives or muscle relaxants.
EP1666883A1 Diagnostic and monitoring methods for bone loss Methods of treating and preventing bone loss and/or enhancing bone formation are disclosed. The methods utilize 15-lipoxygenase inhibitors. These molecules can be delivered alone or in combination with agents which inhibit bone resorption or additional agents that regulate calcium resorption from bone or enhances bone accumulation. The invention additionally provides methods of diagnosing a predisposition to bone loss.
CN102250003A Sinomenine sulfonic acid compound and its preparation and application The invention relates to the field of pharmaceutical synthesis and specifically provides a sinomenine sulfonic acid compound and its preparation and application. The molecular formula of the sulfonic acid compound is C19H25SNO7 with the molecular weight being 411; and the physical and chemical properties are as follows: the sulfonic acid compound is a white powder, is easy to dissolve in water, and can be dissolved in methanol and ethanol. The preparation of the sinomenine sulfonic acid compound comprises the following concrete steps of: mixing sinomenine with one or more components selected from the group consisting of sulfurous acid, sulfite, sulfur dioxide, pyrosulfurous acid, pyrosulfite or thiosulfate to make the mol ratio of sinomenine to sulfite ions in the solution to be 1: 10-8, adding water 6-10 times the weight of the raw material solid substances, heating to react for 4.5-5.5 hours, followed by recrystallization to obtain the sinomenine sulfonic acid compound. The sinomenine sulfonic acid compound has the efficacy of resisting inflammation and releasing pains, and has a better activity than sinomenine.
CA2342064C Long wave length absorbing bacteriochlorin alkyl ether analogs Novel compounds that either preferentially absorb into hyperproliferative tissue and absorb light efficiently at a wavelength of between about 700 and about 850 nm. or act as intermediates for such absorbing compounds. More particularly, the compounds of the invention have the formula: (see formula I) where R1, R5, R9, and R10 are independently lower alkyl of 1 to 3 carbon atoms provided that at least three of R1, R5, R9, and R10 are methyl; R2 is -OH, - OR11, -NHR11, aryl, or -aminoacid; R3 and R4 are independently -COR11 or taken together are (see formula II) R6 and R7 are independently lower alkyl of 1 to 3 carbon atoms; R8 is O-alkyl of 1 to about 12 carbon atoms, S-alkyl of 1 to about 12 carbon atoms, aryl, or a heterocyclic ring of 5 or 6 carbon atoms; R11 is alkyl of 1 to 6 carbon atoms; and R12 is lower alkyl of 1 to about 12 carbon atoms, aryl, or aminoalkyl of 1 to 8 carbon atoms; provided that at least one of R8, R11, and R12 is hydrophobic and together contain at least 10 carbon atoms. The invention also includes method of making and using the compounds.
CN103520199A Application of lycium barbarum polysaccharide in diabetes treating medicine Provided is an application of lycium barbarum polysaccharide in diabetes treating medicine. The diabetes treating medicine is the lycium barbarum polysaccharide extracted and purified from dried lycium barbarum. The study of the chronobiology shows that the concentration of human body insulin and blood sugar changes according to the circadian rhythm, 24h blood sugar monitoring shows that the concentration of blood sugar is the lowest at 3 am, the concentration of blood sugar is the highest at 1 pm or 2 pm, and glucose resistance tests also show daily rhythmicity. The sensitivity of the human body of either a healthy person or a diabetics to insulin and hypoglycemic agents has daily rhythmicity. The human body is most sensitive to insulin at 5-9 am. Tests and studies show that the concentration of blood sugar of an old diabetes rat can be better lowered by medicine feeding at 9 am, insulin is improved to resist rat hyperinsulinemia, toxic and side effect is avoided, using is convenient, price is low, and wide development prospect is achieved.
CN103509013A Salts of delta 11,12-antofine derivatives The invention relates to fumarates of delta 11,12-antofine and delta 11,12-antofine derivatives or pharmaceutically acceptable solvates thereof, and an application of the fumarates or the solvates in preparing drugs for treating cancers.
US20080200402 Use Of Fumagillin And The Derivatives Thereof To Increase The Bioavilability Of The Macrocyclic Lactones The invention relates to the use of fumagillin and the analog derivatives thereof, as inhibitors of cellular transporters, such as ABC transporters, and especially of P-glycoprotein, in order to increase the bioavailability of active ingredients that can be used in the treatment of pathologies such as cancers or parasitic diseases, and especially in order to increase the bioavailability of the macrocyclic lactones.
WO2010068863A3 Pyrimidine compounds and methods of making and using same Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.
CN103191120A Application of pyrimidine derivative in preparation of drugs capable of prevention and/or treatment and/or adjuvant therapy of tumors The invention discloses application of a pyrimidine derivative in preparation of drugs capable of prevention and/or treatment and/or adjuvant therapy of tumors. The pyrimidine derivative comprises a pyrimidine compound having a structural formula (I), a pharmaceutically acceptable salt thereof, a solvate, a polymorphic substance, a tautomer and a prodrug or a composition containing the pyrimidine compound. The structural formula (I) is described in the specification. According to the invention, the novel pyrimidine derivative with Aurora kinase inhibition activity is formed through different C-N couplings and introduction of different pharmacophores respectively at positions 2, 4 and 6 of a pyrimidine ring, and the pyrimidine derivative can be used for preparation of drugs capable of prevention and/or treatment and/or adjuvant therapy of tumors.
US7579342 Pteridine compounds for the treatment of psoriasis The invention provides pteridine compounds of formula (I), processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. Formula (I) in which A is a group of formula (a) or (b).
US7482138 PAK5-related compositions and methods This invention provides nucleic acids encoding human PAK5-related proteins, and provides the encoded proteins. This invention also provides vectors, cells and compositions. Finally, this invention provides methods of inducing and inhibiting various cellular processes using the instant nucleic acids and proteins.
EP1403251B1 Bis(2-aryl-5-pyridyl) derivative A bis(2-aryl-5-pyridyl) derivative represented by the general formula (1): (1) [wherein A represents an optionally substituted aromatic hydrocarbon group and X represents a group selected among the following formulae (2) to (4): (2) (3) (4) (wherein in the formula (2), R1 represents hydrogen or lower alkyl substituted by di(lower alkyl)amino and m is a number of 1 or 2; in the formula (3), Y1 and Y2 each represents nitrogen or CH and n is a number of 0 to 6; and in the formula (4), R2 and R3 each represents hydrogen or lower alkyl, Z represents a single bond, substituted methylene, substituted imino, oxygen, or cycloalkylene, and p and q each is a number of 0 to 6)] or a salt of the derivative. The compound (1) has excellent IgE antibody production inhibitory activity and is useful as a medicine such as a preventive/remedy for allergic immunopathy.
US20100247478 Method for stabilizing vertebral body architecture A method for reducing the occurrence of new post-operative fractures in vertebrae of a patient's spine after a vertebroplasty procedure performed to stabilize a fracture in a vertebra of a patient comprising the steps of performing a vertebroplasty procedure to stabilize a fracture in a vertebra of the patient, wherein the vertebroplasty procedure comprises the step of injecting a material into the fractured vertebra, wherein the material is formed by mixing together a first paste and a second paste, wherein the first paste comprises at least one of a polymerizable monomer and a filler, and wherein the second paste comprises at least one of a polymerizable monomer and a filler.
CN102327273A Compound clobetasol propionate nano-medicament and preparation method thereof The invention discloses a compound clobetasol propionate nano-medicament of which the particle size is 1-100 nanometers. The medicament consists of the following components in percentage by weight: 10.0-50 percent of surfactant, 0-8 percent of cosurfactant, 0.5-20 percent of oil, 0.001-4.0 percent of amitraz, 0.001-4.0 percent of clobetasol propionate, 0.001-10 percent of terbinafine and the balance of distilled water, wherein the total percentage by weight of the components is 100 percent. The medicament has the effects of resisting bacteria, diminishing inflammation, relieving itching and pain, killing mites and treating fungal diseases, eczema and various types of dermatitis caused by fungi such as dermatophyte, microsporosis capitis, acrothesium floccosum, microzyme of monilia and chaff ringworm fungus, and the like. The medicament is a yellow or colorless clear transparent liquid and has the advantages of high stability, high wetting property, good transdermal effect, nontoxicity, non-irritation, high safety, easiness for preparing, low cost and convenience for popularizing.
WO2006028160A1 S-oligonucleotide conjugate and antisense agent A novel conjugate which has high activation inhibitory activity especially against the telomerase contained in a human leukemic cell extract and which gives a stable duplex hybrid with a complementary DNA. It is a phosphorothioate oligonucleotide conjugate represented by the general formula [Chemical formula 1] (wherein A1 is alkylene or alkylene separated by an oxygen atom; A2 is alkylene; R is a residue of a peptide, sugar, or functional amine; and n is 0 or 1). Also provided is an antisense agent containing the conjugate as an active ingredient.
WO2012031196A1 4- { [ ( pyridin- 3 - yl -methyl) aminocarbonyl] amino} benzene - sulfone derivatives as nampt inhibitors for therapy of diseases such as cancer The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
US20120259020 Transdermal therapeutic systems containing 4-n-butylresorcinol Transdermal therapeutic systems that contain 4-n-butylresorcinol as an active ingredient.
CA2326356C Oral liquid antidepressant solution For the oral administration of the anti-depressant mirtazapine an aqueous solution or suspension is found which is preferably stabilised by methionine, is thickened, and which has a pH of from 2.5 to 3. By the formulation according to the invention, an undesirable local anaesthetic effect of mirtazapine is avoided.
US20050009682 Antimicrobial alkali-silicate glass ceramic and the use thereof The invention relates to a glass ceramic, wherein the initial glass comprises 30-65 percent (by weight) SiO2; 5-30 percent (by weight) Na2O; 5-30 percent (by weight) CaO, and 0-15 percent (by weight) P2O5, and wherein the main crystalline phases comprise alkali-alkaline earth-silicate and/or alkali silicate and/or alkaline earth silicate. The invention is characterized in that either a glass ceramic with a single crystalline phase 1 Na2O-2 CaO-3 SiO2 is excluded, or the crystalline size of the glass ceramic is <10 μm, or the weight fraction of SiO2 is <47%.
WO2011036561A8 Process Substantially pure methylthioninium chloride pentahydrate form A is prepared from methylthioninium chloride by phase equilibration of suspensions, crystallization or solvent evaporation, whereby the water content of the solvent corresponds to a water activity of at least 0.4 at 25°C, and controlled drying of said methylthioninium chloride pentahydrate form A within its stability ranges of humidity, pressure and temperature.
WO2008002629A1 Process for the preparation of zopiclone Provided is a process for the preparation of zopiclone, an intermediate in the synthesis of eszopiclone. The present invention provides a process for preparing zopiclone by combining 6-(5-chloro-2-pyridinyl]-6,7-dihydro-7-hydroxy-5H-pyrroIo[3,4-b]pyrazine-5-one (7-OH-Py) having the formula (I), with chloro-carbonyl-4-methyl-piperazine (CMP) as a free base or an acid addition salt having the formula (II), 4-N,N-dimethylamino-Pyridine (DMAP) catalyst and a base in the presence of a polar solvent.
CN1582760A Nucleotide and amino acid nutrient products and their production A composite nutrient for increasing the ability to synthesize nucleic acid, improving immunity and resistance to disease and fatigue, and delaying senility is prepared from composite nucleotide, composite amino acid, and composite methyl chemical. It can be used for food, beverage, flavouring, cosmetics and medicine.
EP2043648A1 Use of flibanserin for the treatment of sexual disorders in females The invention is directed to the use of flibanserin or a pharmacologically acceptable derivative thereof, for the preparation of a medical composition for the treatment of Sexual Disorder in females whereby the medication of a patient is selected to achieve a significant change (with administration of a therapeutically effective amount of flibanserin) starting from a baseline (without administration of flibanserin), the significant change being achieved within at least one primary criteria for efficacy and optionally within at least one secondary criteria of efficacy.
CN101669912A Slow-release composition containing tamsulosin and preparation thereof The invention provides a slow-release composition containing tamsulosin and preparation thereof; and a slow-release micro-pill preparation which is prepared by adding a certain thinning agent and retarding agent has the release rate being consistent with the need.
CN102671191A Composition with high dose of chondroitin sulfuric acid and method for treating type 2 diabetes mellitus The invention relates to the field of the drugs or the nourishments, and specifically relates to a composition with high dose of chondroitin sulfuric acid and a method for treating type 2 diabetes mellitus. The composition is characterized in that the chondroitin sulfuric acid extracted from animals is selected, which contains substances providing nutrition needed by islet cells and is capable of promoting the cells to absorb the nutrition quickly; therefore, the islet cells are capable of enhancing self-regulation capability and then is gradually recovered to play a normal role, and the functions of the insulin are completed; and in this way, the purpose of treating the type 2 diabetes mellitus is achieved. The invention discloses the method for treating the type 2 diabetes mellitus.
CN101190181B Monomer nano silver sanitary tampon and preparation method thereof The invention relates to a monocase nano-silver sanitary suppository and a manufacturing method of the suppository. The invention comprises nano-silver content and basic component. The nano-silver content is the monocase nano-silver, i.e. pure silver monocase of nano size, and the basic component is water solubility component. The weight of the monocase nano-silver accounts to 1 to 2000 ppm of thetotal weight of the suppository. The sanitary suppository of the invention can be used for treating various dermatosis, gynecological diseases and prostate diseases, etc. Compared with the prior art,the sanitary suppository of the invention has the advantages that the sterilization effect is high; after the sterilization, no matter which is harmful for people is generated; the medicine effect ismoderate and durable. The manufacturing method of the monocase nano-silver sanitary suppository of the invention is that monocase nano-silver water solution is prepared first; then the monocase nano-silver water solution is dispersed to the water solubility component. And the solution can be dispersed evenly just by stirring, with a simple manufacturing process.
US20080207697 Nervous system connecting diseases such as autism The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect, such as schizophrenia or autism.
US20110206636 Use of Endoperoxides for the Treatment of Infections Caused by Flaviviridae, Including Hepatitis C, Bovine Viral Diarrhea and Classical Swine Fever Virus The use of sesquiterpenes and, in particular sesquiterpene lactone endoperoxides, such as artemisinin and analogs thereof, for the treatment of hepatitis C virus infections. Artemisinin, analogs of artemsisnin and some crude Artemisia extracts were tested in vitro against DNA-viruses, retro-viruses and Flavivirida, (an important family of human and animal RNA pathogens). These compounds were also screened for anti-tumor activity. Strong activity of artemisinin was noticed against the bovine viral diarrhea virus (BVDV). As pestiviruses, such as BVDV, share many similarities with hepatitis C virus (HCV), we can conclude that endoperoxides in general and artemisinin more specifically have efficacy as treatments for hepatitis C viral infections.
US20050032861 Antibiotic (vancomycin) resistant Grampositive and Gramnegative bacteria; cycloadditon, reduction, coupling, salt formation, deprotecting, amination, oxidation Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an N-linked 5-membered, fully or partially unsaturated heterocyclic ring, or an N-linked 6-membered di-hydro-heteroaryl ring; and Q is, for example, Q1 or Q2: wherein R2 and R3 are independently hydrogen or fluoro; T is selected, for example, from a group of the formula (TA1) or (TA2): wherein, for example, X1m is O═ and X2m is R2s—(E)ms—N—; wherein E is an electron withdrawing group, for example, —SO2— or —CO—; and, for example, R2s is hydrogen or (1-6C)alkyl; are useful as pharmaceutical agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
CA2258895C Use of topiramate or derivatives thereof for the manufacture of a medicament for the treatment of manic-depressive bipolar disorders Anticonvulsant derivatives useful in treating Manic-depressive disorder are disclosed.
CN1989997A Drop pill for treating pharyngitis and its preparation method The invention relates to a dripping pill for treating pharyngitis and its preparing process, wherein the medicament is prepared from glabrous sarcandra herb extract, natural boneol and menthol through steps of ethanol extracting glabrous sarcandra herb, drying into fine powders, heating base material till melting, charging the fine powders while stirring, charging into natural boneol and menthanol, and making dripping pills under condition of thermal insulation.
WO2004056307A3 Disease treatment via antimicrobial peptide inhibitors A method of treating a disease in a subject in need thereof is disclosed. The method comprises providing to the subject a therapeutically effective amount of a compound being capable of decreasing an activity and/or level of an antimicrobial peptide (AMP) and/or AMP-like molecule, thereby treating the disease in the subject in need thereof.
EP1274710B1 Novel heteroaryl-diazabicycloalkanes The present invention relates to novel heteroaryl-diazabicycloalkanes which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
WO2009042733A1 Solids forms of ( s) -ethyl 2-amin0-3- (4- (2 -amino- 6- ( (r) -1- (4-chl0r0-2- o-methyl-ih-pyrazol- 1-yl) phenyl) -2, 2, 2-trifluorethoxy) -pyrimidin-4-yl) phenyl) propanoate Solid forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate and salts thereof are disclosed.
CN103333138A Novel Cabazitaxel crystal form, preparation method, application and pharmaceutical compositions thereof The invention provides a novel Cabazitaxel crystal form, a preparation method, application and pharmaceutical compositions thereof. As the novel Cabazitaxel crystal form provided by the invention is lower in solvent residue, the phenomena that compositional variation or crystal form transformation occurs due to a solvent can be easily removed during a process that a Cabazitaxel solvate is heated or is stored for a long term and amorphous Cabazitaxel is easy to absorb moisture during a long-term storage process are avoided, and the stability of Cabazitaxel is improved. Proved by research results, the novel Cabazitaxel crystal form is not easy to generate the crystal form transformation. Meanwhile, the preparation method provided by the invention is simple to operate, and complicated crystallization conditions are avoided. The novel Cabazitaxel crystal form, the preparation method, the application and the pharmaceutical compositions thereof are more suitable for industrial applications.
CN102274191B Pharmaceutical composition erythromycin enteric-coated pellet capsule The invention provides an erythromycin enteric-coated pellet which is suitable to be prepared by a boiling coating granulator, wherein the enteric-coated coating liquid comprises polyacrylic resin II, diethyl phthalate, tween-80, and an ethanol solution. In addition, the invention also provides a process and an intermediate material for preparing the erythromycin enteric-coated pellet, such as enteric-coated coating liquid and the like.
US20060111354 Medicaments containing vardenafil hydrochloride trihydrate The invention relates to a method for producing medicaments that contain vardenafil hydrochloride, essentially as trihydrate in solid form, and to medicaments that can be obtained according to this method
US20070066578 5-Aminosalicylic acid solid preparation improved in discoloration and method of storing the same It is an object of the present invention to inhibit browning of a 5-aminosalicylic acid solid preparation, and to maintain for an extended period the properties of the 5-aminosalicylic acid solid preparation the same as they were at the time of the manufacturing the preparation. The present invention provides a solid preparation obtained by formulating 5-aminosalicylic acid or a salt thereof and a discoloration inhibitor into a drug product, wherein this solid preparation exhibits a color difference in a CIELAB color space being 10.5 or less before and after storage at 80° C. for one week. The above-mentioned discoloration inhibitor contains at least one selected from the group consisting of a thiol compound, a sulfide compound, an acid anhydride, and a hygroscopic compound.
EP1783128A1 Heterocyclic compounds and their use as antifouling agents The present invention relates to a nostocarboline compound of the formula (I) and its use as a biocidal agent. In this formula R1, R3, R4 and R6 are selected from the group consisting of H, F, Cl, Br, I, a C1-C20 aliphatic residue, and a C1-C20 aliphatic residue comprising a carbocyclic or heterocyclic residue; R2 is selected from the group consisting of H and Cl; R5 is selected from the group consisting of H, a C1-C20 aliphatic residue, and a C1-C20 aliphatic residue comprising a carbocyclic or heterocyclic residue; R7 is selected from the group consisting of a C1-C20 aliphatic residue, a C1-C20 aliphatic residue comprising a carbocyclic or heterocyclic residue, and a linker bound to a bioactive factor; R8 is selected from the group consisting of H, a C1-C6 aliphatic carboxylic acid, ester, or amide, and a C3-C20 carbocyclic residue; and X- is a negatively charged ion.
EP1668985A2 Nucleophile substituted ecteinascidins and N-oxide ecteinascidins Five new nucleophile substituted ecteinascidin compounds were isolated from extracts of Exteinascidia turbinata and designated Et 802, Et 788, Et 760, Et 858 and Et 815. Three new N-oxides were also obtained and designated Et 717, Et 775 and Et 789. Some of these newly discovered Et compounds show exceedingly potent cytotoxicity against L1210.
CA2478138A1 Cxcl10-based diagnosis and treatment of respiratory illnesses Elevated blood levels of the chemokine CXCL10 polypeptide are associated with respiratory illnesses (e.g. SARS, influenza and community-acquired pneumonia) and are useful in diagnosis of patients. Methods are provided for diagnosis and treatment of patients suffering from respiratory illnesses. Methods are provided for identifying inhibitors of the CXCL10:CXCR3 axis, for use in treating patients suffering from respiratory illnesses.
DE102007028198A1 New alkyl-ketone compounds are histone deacetylase inhibitors, useful to treat e.g. cancer, hematologic or solid tumors, non-Hodgkins tumors, T-cell lymphoma, type I diabetes or Hashimoto's thyroiditis, and to modulate e.g. cell cycle Alkyl-ketone compounds (I), are new. Alkyl-ketone compounds of formula (Ar1-[CH 2] m-Z 1>-N(Z 2>-R 2>)-Z 3>-[CO] r-[CH 2] n-Y 1>-[CO] s-Y 2>-R 1>) (I), are new. Ar1 : benzyl, aryl- or heteroaryl (all containing 1-3 substituents of -F, -Cl, -1-4C alkyl, -OH, -O-1-4C alkyl, -CF 3 or -NH 2); Z 1>-Z 3>a direct bond, O or S; Y 1>, Y 2>a direct bond, N(-R 2>), - N(-R 2>)-O-, -O-N(-R 2>), O or S; n : 1-10; m : 0-4; r, s : 0 or 1; R 1>benzyl- or (hetero)aryl residue (both containing 1-3 substituents of -F, -Cl, 1-4C alkyl, -OH, -O-1-4C alkyl, -CF 3- or -NH 2); and R 2>H or 1-4C alkyl. - ACTIVITY : Cytostatic; Antianemic; Antiapoptotic; Apoptotic; Angiogenesis Modulator; Antiinflammatory; Antiasthmatic; Antiallergic; Ophthalmological; Dermatological; Antiarthritic; Osteopathic; Vasotropic; Antirheumatic; Gastrointestinal-Gen; Antibacterial; Immunosuppressive; Antidiabetic; Hemostatic; Neuroprotective; Muscular-Gen; Antipsoriatic; Nephrotropic; Respiratory-Gen; Immunomodulator; Anabolic; Cardiant; Nootropic; Tranquilizer; Anticonvulsant; Neuroleptic. - MECHANISM OF ACTION : Histone deacetylase inhibitor; Dipeptidyl peptidase IV inhibitor.
WO2007136326A3 ) t e text as een esta s e y t s ut o ty to rea as o ows: 1- [ (4- [benzoyl (methyl) amino] -3- (phenyl) butyl] azetidine derivatives for the treatment of gastrointestinal disorders 3 The present invention relates to novel 1- [ (4- [3-chloro-5- (trifluoromethyl) benzoyl (methyl) amino] -3- (4- fluorophenyl) butyl] -3-morpholin-4-yl-azetidine derivatives, as well as salts and enantiomers thereof. The invention also relates to pharmaceutical compositions comprising said compounds, and to the use of said compounds in therapy, e.g. in the treatment of gastrointestinal disorders. The invention further relates to processes for the preparation of the compounds. The compounds are neurokinin (NK) receptor antagonists.
WO2008036841A2 Tripartite oligonucleotide complexes and methods for gene silencing by rna interference Provided herein are tripartite oligonucleotide complexes which can be administered to a cell, tissue or organism to silence a target gene. The tripartite oligonucleotide complexes of the disclosure may include a conjugate moiety that facilitates delivery to a cell, tissue or organism without the aid of a transfection reagent.
CN103596563A Methods for regulating Sirtuin gene expression The invention provides methods useful for regulating sirtuin gene expression, mimicking caloric restriction, preventing and treating Alzheimer's disease, increasing longevity and retarding aging in an animal. The methods comprise administering one or more isoflavones to the animals, preferably in amounts of from about 0.001 to about 10 g/kg/day.
US20080014255 Liposome bonded with antibody and polyalkylene glycol A liposome wherein a compound containing a polyalkylene glycol moiety is bonded through a thioether group and an antibody is bonded through a thioether group to a liposome comprising lipids whose partial component has maleimidated terminal, wherein an amount of the bonded compound and an amount of bonded antibody is 15 to 50 mole % and 0.1 to 2 mole %, respectively, based on one mole of the maleimidated lipid contained in the liposome. The liposome achieves both excellent blood retention and therapeutic effect.
WO2011065545A1 5-FLUOROURACIL COMPOUND HAVING dUTPase-INHIBITING ACTIVITY OR SALT THEREOF A 5-fluorouracil compound represented by general formula (I) or a salt thereof, which has an excellent dUTPase-inhibiting activity and is useful as an efficacy potentiator for anti-tumor agents or the like. (In general formula (I), n represents a numeral value of 1 to 3; X represents a bond, an oxygen atom, a sulfur atom, an alkenylene having 2 to 6 carbon atoms, a bivalent aromatic hydrocarbon group which may have a substituent, or a bivalent saturated or unsaturated heterocyclic group which may have a substituent; Y represents a bond, or a linear or branched alkylene group having 1 to 8 carbon atoms; Z represents -SO2NR1R2, -NR3SO2-R4, or a group represented by formula (II) (a R5-substituted pyrrolidinylcarbonyl); R1 and R2 independently represent a hydrogen atom, or the like; R3 represents a hydrogen atom, or the like; R4 represents an aromatic hydrocarbon group which may have a substituent, or the like; and R5 represents a methyl group which may have a substituent.)
US20100099760 Glycyrrhetinic Acid Derivatives The present invention relates to novel derivatives of glycyrrhetinic acid, compositions comprising said derivatives and their use in the treatment of conditions or diseases that benefit from an upregulation of PPAR&ggr; and/or a downregulation of the expression or activity of one or more specificity (Sp) proteins, such as cancer, diabetes and Huntington's disease.
EP2414372A1 Chemical synthesis of phosphatidylinositol mannoside glycans from mycobacterium tuberculosis The efficient synthesis of phosphatidylinositol mono- to hexa-mannoside (PIM1 to PIM6) is reported. The invention relates to these phosphatidylinositol mono- to hexa-mannosides carrying a linker and a reactive functional group, e.g. the sulfhydryl group, a protein, a fluorescent probe, or a solid phase. The invention further relates to vaccines comprising the PIMs linked to a carrier protein or an antigen
US20120108668 Metabolic profiles The invention relates to the use of endogenous metabolites to produce a metabolic profile of a disorder or disease in a subject, e.g. an autoimmune disease, in particular rheumatoid arthritis, and the analysis of such metabolic profiles in order to find disturbances in such profiles in a subject which are caused by or correlated with the said diseases or disorders. Such disturbances can be normalised by treatment of the subject with specified compounds, particularly N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine or an aminoguanidine.
EP2170828A1 Substituted n-aryl pyridinones as fibrotic inhibitors Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
CN102475712A Pharmaceutical composition used for preventing and treating diabetes and its complications The invention provides a pharmaceutical composition used for preventing and treating diabetes and its complications, the pharmaceutical composition comprises an ophiopogon japonicus polysaccharide extract, element chromium and an excipient which can be taken as the effective components. The ophiopogon japonicus polysaccharide extract is a water extract or a water-containing alcohol extract of ophiopogon root. The chromium is chromium salt, preferably chromium picolinate. In the pharmaceutical composition, the ratio of ophiopogon japonicus polysaccharide extract to chromium is 50000:1-1000. The pharmaceutical composition of the present invention has the effects of insulin resistance reduction and substantial hpyerglycemic effect, especially is capable of reducing blood fat and blood sterollevel, and minimizing and improving the complications of diabetes.
US20050090496 Sulphonyl compounds with 5-ht6 receptor affinity The present invention relates to novel sulfonamide compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.
CN103251586A Anticancer composition based on anti-angiogenesis medicine Aiming at the prior art, the invention aims to provide an anticancer composition based on an anti-angiogenesis medicine. The anticancer composition comprises a vascular endothelial growth factor receptor protein kinase inhibition medicine, namely a VEGFR inhibition medicine; and furthermore, according to the characteristic of a molecular passageway, a targeted medicine deoxyverrucosidin and a medically accepted carrier or excipient thereof are selected to be combined with the VEGFR inhibition medicine and a medically accepted carrier or excipient thereof, so that the problem of medicine resistance of the VEGFR inhibition medicine is fundamentally solved; and the effect of treating cancers is greatly enhanced.
US20120302519 Multiple substituted fluoromethanes as selective and bioactive isosteres Disclosed herein are substituted fluoromethanes; pharmaceutical compositions comprising a therapeutically effective amount of the same; processes for preparing these fluoromethanes; and methods of using the same in alleviating infection and parasitism. Also disclosed are methods for identifying substituted fluoromethanes for modulating the activity of receptors and enzymes that bind and/or modify phosphate containing ligands and substrates.
CN102225187B Cacumen biotae and golden cypress blood-stasis-dissipating paste and preparation method thereof The invention discloses cacumen biotae and golden cypress blood-stasis-dissipating paste and a preparation method thereof. The cacumen biotae and golden cypress blood-stasis-dissipating paste is prepared from the following raw materials by weight: 50-70g of rheum officinale, 40-55g of cacumen biotae, 30-40g of golden cypress, 30-40g of curcuma zedoary, 30-40g of turmeric, 30-40g of rhizome sparganii, 30-40g of mint, 30-40g of herba fibraureae recisae, 30-40g of herba lycopi, 30-40g of lotus leaves, 30-40g of seaweed, 30-40g of radix zanthoxyli, 20-30g of jasmine, 20-30g of flemingia philippinensis, 20-30g of tenuifolia, 20-30g of talc, 10-20g of borneol, 6-15g of cassia twig, 6-15g of cynanchum paniculatum, 6-15g of strychnos alkaloids, 6-15g of notopterygium root and 3-10g of peach kernel. The cacumen biotae and golden cypress blood-stasis-dissipating paste has the effects of promoting blood circulation and removing blood stasis, clearing away heat and toxic materials, detumescence and relieving pain and the like, mainly treats pain, turgidness and the like caused by qi stagnation and blood stasis and heat-toxin, and is mainly used for treating acute and chronic uterine inflammation.
US20070104719 Caspase Activated Prodrugs Therapy The invention provides novel method for the localized delivery of pharmaceutical agents by the administration of a caspase conjugate that targets a cell type of interest and the additional administration of a pro-agent that is locally converted, in the presence of the caspase, to an active agent. The invention further provides novel tageting agents comprising a caspase as well as novel prodrugs comprising a caspase cleavable prodrug moiety. The invention also provides pharmaceutical compositions as well as methods of treatment comprising the caspase conjugates and prodrugs of the invention
WO2012139487A1 Pegylated derivatives of camptothecin compounds The present invention relates to pegylated derivatives of camptothecin compounds, the preparation method therefor, pharmaceutical compositions comprising same, and the uses thereof against tumors.
CN103704817A Wild blueberry juice beverage with cancer resistant effect and making method thereof The invention discloses wild blueberry juice beverage with a cancer resistant effect and a making method of the wild blueberry juice beverage. The wild blueberry juice beverage is prepared from the following components in percentage by weight: 8-15 percent of wild blueberry juice, 10-15 percent of white granulated sugar, 1.20-1.50 percent of honey, 1.00-1.65 percent of malic acid, 0.005-0.016 percent of pectinase, 0.01-0.04 percent of gelatin, 0.80-1.80 percent of camptotheca acuminate, 0.60-1.20 percent of crotalaria sessiliflora, 0.40-0.60 percent of figs, 0.20-0.40 percent of cobra and the balance of water. According to the wild blueberry juice beverage, the wild blueberry juice is used as a main raw material; the wild blueberry juice beverage is obtained by mixing and stewing as well as finely filtering effective active components which are extracted from the camptotheca acuminata, the crotalaria sessiliflora, the figs and the cobra and have the cancer resistant effects; the sour, sweet and delicious beverage is used as a carrier and is extremely easy to absorb by a human body; mutual benefiting can be realized, and the effect is enhanced.
EP1338281B1 Method for producing an immunotropic antiviral preparation The invention relates to the chemical pharmaceutical industry, in particular to a method for producing an immunotropic preparation exhibiting a high antiviral activity with respect to RNA and DNA viruses. In order to produce the inventive preparation, fat-free sturgeon or salmon milt, or a calf thymus, or chicken blood, or porcine liver is pulverised and homogenised in a saline citrate solution. The produced homogenate is incubated in the presence of a detergent, a calcium chlorine solution being added at a high temperature. Afterwards, said homogenate is treated by ultrasound, a sorbent and detergent and concentrated, thereby producing a white amorphous deposit of DNA which has the following characteristics: a molecular mass ranging from 270 to 500 kD, a hyperchromatic action not less than 37 %, a protein content of less than 1 %. The DNA deposit is dried and the obtained powder is diluted in an aqueous solution of the following transition metal: Zn, Co, Mn, Sb, whereby a 1.5 % sterilised solution having a hyperchromatic action equal to or higher than 10 % is obtained.
WO2010039654A3 Topical treatment of skin infection The invention relates to an unexpected discovery that propylene glycol is highly effective at killing or inhibiting Propionibacterium acnes in a mammalian skin disorder, as well as to the use of propylene glycol and salicylic acid in a skin- disorder treatment. This invention also relates to compositions containing propylene glycol alone or in combination with salicylic acid for use in killing or inhibiting Propionibacterium acnes.
US20100022556 Therapeutic combinations comprising a long acting dihydropyridine calcium-channel blocker and a statin A medicament comprising (±)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-[4-(diphenylmethyl)-1-piperazinyl]ethyl methyl ester (manidipine) or a physiologically acceptable salt and a statin or a physiologically acceptable salt.
US20090042943 Benzoyl-piperidine derivatives as dual modulators of the 5-ht2a and d3 receptors The present invention relates to compounds of formula (I) wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
WO2013182551A1 Saccharide fraction from wheat, isolation process and field of use of the invention Fractions extracted from wheat seeds germinated and macerated in water having a molecular weight comprised between 3 and 30 K Daltons are described.
EP1064274B1 Benzenesulfonamide derivatives and their use as medicaments Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R?1 and R2¿ are substituents as defined within; R?3 and R4¿ are defined within and are alkyl or halo alkyl or together form a cycloalkyl or halocycloalkyl ring; R5 is a substituent as defined within; Y-Z is a linking group as defined within; are useful in the production of an elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.
CN1634060A Gelatin formulation of dextromethorphan hydrobromide and its preparing method The invention provides a gelatin formulation of dextromethorphan hydrobromide and its preparing method, which is prepared from acetaminopher, chlorpheniramine maleate, d-pesudoephedrine hydrochloride, Dextromethorphan Hydrobromide and right amount of base material, The preparation is in the form of gel type oral form, the process for preparing the preparation is also disclosed. The children are willing to take the preparation, it has good effects for controlling children's virus infection of upper respiratory tract and treating children's common cold.
CN103417766A Medicine for treating juvenile parotitis The invention provides a medicine for treating juvenile parotitis. The medicine comprises the following component in parts by weight: 8-16 parts of rhizoma coptidis, 6-12 parts of fructus gardeniae, 6-12 parts of rheum officinale, 8-16 parts of prunella vulgaris, 1-5 part(s) of borneol, 6-12 parts of amur cork tree bark, 10-15 parts of radix scutellariae, 8-16 parts of rhizoma acori graminei, and 9-12 parts of liquorice. The medicine for treating juvenile parotitis has the advantages and the positive effects of remarkable treatment effect and low cost.
CN101366724A Filling liquid after uterine lumen surgery The invention relates to a filling solution used after a uterine cavity operation, which is characterized in that the compositions of the filling solution as calculated by 100 milliliters are 0.05 to 2.0 grams of sodium hyaluronate, 0.01 to 2 grams of antibiotic, 10 to 20 milligrams of local anesthetic and the balance being physiological saline. The filling solution can effectively prevent and treat the problems of pain, infection, adhesion and so on after the uterine cavity operation, and simultaneously reinforces the function of other medicines and reduces the probability of generating untoward reaction due to the existence of the sodium hyaluronate.
US20120172751 Assessment and Modulation of Cerebrospinal Fluid for Head Pain The disclosure relates to the discovery that certain cerebrovascular disorders in humans who exhibit seemingly normal intracranial pressure (ICP) and do not exhibit hydrocephalus can be alleviated or prevented by reducing ICP in the human. Disorders of this type are herein designated normotensive, nonhydrocephalus tenso-responsive cerebrovascular disorder (NNTCDs). The disclosure describes methods of relieving head pain and other symptoms of NNTCDs, for example by withdrawing cerebrospinal fluid (CSF) from the subarachnoid space of a human or by administering a pharmaceutical agent that modulates CSF production, uptake, or both. Methods of assessing whether a human is afflicted with one or more NNTCDs are also described. The disclosure describes numerous pharmaceutical compositions suitable for administration to humans afflicted with NNTCDs to alleviate or prevent such disorders. Such compositions can, for example, include both a CSF-reducing agent and a symptomatic (e.g., head pain) relief agent.
WO2007001839A3 4-anilino-3-quinolinecarbonitriles for the treatment of cancer The present invention is directed to a method of preventing treating and/or inhibiting cancer using compounds of formula (I): or a pharmaceutically acceptable salt thereof. This invention is also directed to pharmaceutical compositions containing compounds of formula (I).
CN1813734A Procaterol hydrochloride dropping pill and its preparing method The present invention discloses a medicine procaterol hydrochloride dipping pills preparation with the action of relieving asthma and its preparation process. It is made up by using procaterol hydrochloride and matrix for making dripping pills.
CN102000103A Medicinal application of 2'-fluoro-4'-nitrine-nucleoside analogues or salt thereof The invention discloses a medicinal application of 2'-fluoro-4'-nitrine-nucleoside analogues, belonging to the field of pharmaceutical chemistry. The nucleoside analogues has the following structure and is used for preparation antineoplastic drugs for treatment of intestinal cancer, liver cancer, gastric cancer, esophageal cancer, lung cancer, breast cancer, cervical carcinoma, leukocythemia, lymphadenoma and the like, and has better activity and lower toxicity side effect, so that the medicinal application has good development and application foreground.
US20110071117 Combinations of antioxidants and anti-inflammatory drugs in the treatment of inflammatory bowel disease Disclosed herein are compositions comprising 5-aminosalicylic acid (5-ASA), or a pharmaceutically acceptable salt thereof and an antioxidant, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating an inflammatory bowel disease in a subject, reducing cytokine gene expression in colonic tissue of a subject, and reducing myeloperoxide activity in colonic tissue of a subject, comprising administering to the subject a therapeutically effective amount of a composition comprising 5-ASA, or a pharmaceutically acceptable salt thereof, and an antioxidant, or a pharmaceutically acceptable salt thereof.
US20050249831 Herbal extract comprising a mixture of saponins obtained from sapindus trifoliatus for anticonvulsant activity A pharmaceutical composition comprising a herbal extract, comprising a mixture of saponins prepared from the pericarp of Sapindus trifoliatus, with binding affinities for the receptor sites viz. GABA-A agonist site, Glutamate-AMPA site, Glutamate-Kainate site, Glutamate-NMDA agonistic site, Glutamate-NMDA glycine (strychnine insensitive) site and Sodium channel (site 2), having major mediatory role in anticonvulsant activity. A process for preparation of the herbal extract; isolation of six pure compounds from the mixture of saponins in the aqueous extract; and a pharmaceutical composition comprising the said extract in combination with pharmaceutically acceptable additives. A method of prophylactic treatment of migraine through anticonvulsant activity of the composition by its administration through intranasal route.
US20050020523 Modified antisense nucleotides complementary to a section of the human haras gene The invention relates to a specific modified oligonucleotide complementary to a section of the human Ha-ras gene and mRNA, and its use to specifically regulate, modulate or inhibit expression of the HA-ras gene, and its use as a pharmaceutical for the treatment of conditions arising from the abnormal expression of the Ha-Ras gene, in particular in combination with chemotherapy and radiotherapy. The modified oligodeoxynucleotide according to the invention has the sequence 5′-TxAxTxTxCxCxGxTxCxAxT-3′-O—PO2—O—R (SEQ ID NO:1), wherein X is an internucleotide linkage of type o or s, with the proviso that x is an s linkage at least 4 times and at most 9 times, and o means a phosphodiester internucleoside linkage, s means a phosphorothioate internucleoside linkage, R means a C8-C21 alkyl group, —(CH2—CH2O)n-(CH2)m—CH3, or —CH2—CH(OH)CH2O—(CH2)q—CH3 wherein n is an integer from 1 to 6, m is an integer from 0 to 20 and q is an integer from 7 to 20 and A is 2′-deoxyadenosine, G is 2′-deoxyguanosine, C is 2′-deoxycytidine and T is thymidine.
US20120142580 Opioid receptors stimulating compounds (thymoquinone, nigella sativa) and food allergy The present invention relates generally to the fields of food allergy and nutrition. It was found that the stimulation of opioid receptors could be used to treat or prevent food allergy. One embodiment of the present invention concerns hence the use of an opioid receptor stimulating compound like thymoquinone or plant extracts from Nigella sativa, Eupatorium ayapana, Satureja montana or Thymus for the preparation of a composition to treat or prevent food allergy.
US7303755 Use of sodium and potassium salts of citric, phosphoric, carbonic and tartaric acid and arginine and lysine as stabilizer of the antibiotic Fosfomycin Tromethamine The use of certain salts and aminoacids as stabilizer of the antibiotic Fosfomycin Tromethamol and pharmaceutical compositions containing them, is described.
US7485659 Anticancer compositions, and methods of making and using the same Compositions, containing a ruthenium(III) complex and a heterocycle, methods for their manufacture, medicament containing these compositions and a kit. The invention relates to a composition (A), obtained by reacting a compound of the general formula (I) M3−n−p−2pr[RUX6−n−p−q−2rBn(H2O)p(OH)q(O)r]2r+1 (I) with a compound of the general formula (II) B′(HX′)s (II). Furthermore, the invention relates to a composition (B), obtained by mixing a compound of the general formula (III) (B′H)3−n−p−2pr[RUX6−n−p−q−2rBn(H2O)p(OH)q(O)r]2r+1 (III) with a compound of the general formula (IV) MX′ (IV).
US20080279808 2,3,4,5-Tetrahydroxy-6-Sulfooxy Hexanoic Acid, Pharmaceutically Acceptable Salts and Equilibrium Forms Thereof, Processes for Their Preparation, Pharmaceutical Compositions Comprising Such Compounds and Their Medical Use The invention relates to novel compounds of general formula I wherein M represents hydrogen, or a metallic cation, preferably an alkaline metal, or alkaline-earth metal, and n is equal to 1, 2 or 3. The present invention also comprises compounds of general formula I in their equilibrium forms, including lactonic forms, their enantiomers in pure form, or in an enriched form in one of the optical isomers, racemic mixtures, diastereomers and solvates thereof. The present invention further relates to processes for the preparation of compounds of general formula I, to pharmaceutical compositions comprising compounds of general formula I as only active ingredient, or in association with other active ingredients. Another aspect of the invention is the use of compounds of general formula I for the treatment of dyslipidemia, associated, or not, to other metabolic disorders, such as glucose intolerance syndrome and type 1 or 2 diabetes mellitus, by means of isolated administration or combined with other substances.
CN103301119A Edaravone composition for injection The invention provides an edaravone composition for injection, and relates to the technical field of medicine manufacturing. The main medicine of the composition comprises edaravone and melatonin, wherein the melatonin comprises a quick release part and a cyclodextrin-included slow release part. According to the edaravone composition for injection provided by the invention, the therapeutic effect of edaravone is improved, instability caused by oral administration of MT (Melatonin) is avoided and MT is quick to distribute and eliminate and the like, and the first pass effect of MT is reduced. The dosage of edaravone is reduced, and the side effect of edaravone is reduced. The design of dosage combining quick release and slow release is in accordance with secretion characteristic of MT, so that the problem of half-life period of MT is solved and the bioavailability of a product is improved. The melatonin combined with edaravone acted on nerve cells has the synergistic effect of preventing encephaledema, reducing the infarct volume and improving the neurological function.
WO2011093809A3 Dry powder pharmaceutical composition comprising tiotropium and ciclesonide The present invention relates to pharmaceutical compositions in dry powder form comprising tiotropium and ciclesonide and/or their pharmaceutically acceptable derivatives as active agents, and capsule and blister forms containing these pharmaceutical compositions so as to be used in treatment of respiratory tract diseases.
US20100168050 Compounds having antiangiogenic activity The use of o-ATP as a pharmacological agent useful for the treatment of diseases in whose onset or progression angiogenesis is involved.
EP1904055A1 Composition for inhibiting acyl-coa:cholesterol acyltransferase Disclosed herein is a composition having activity of inhibiting acyl-CoA: cholesterol acyltransf erase, which comprises retrofractamide A, pipercide, piperrolein B, piperchabamide D, pellitorin or combinations thereof, or a pharmaceutically acceptable salt thereof . The composition is effective for preventing and treating vascular diseases, such as hyperlipidemia, arteriosclerosis, etc.
CN103751108A Pranlukast solid dispersion and preparation method thereof The invention relates to pranlukast solid dispersion and a preparation method thereof, belonging to the field of pharmaceutical preparations. Particularly, the invention provides solid dispersion and a pharmaceutical composition. The solid dispersion is composed of pranlukast, a water-soluble polymer and a surface active agent; and the pharmaceutical composition is composed of pharmaceutically acceptable carriers. The solid dispersion disclosed by the invention is capable of increasing solubility of medicines, improving viscidity of pranlukast and prompting absorption, and therefore, dissolution rates and bioavailability of medicines are increased.
WO2008051416A2 Compounds that inhibit the activity of hsp90 for treating infections The present invention relates to compounds for treating or preventing infection that inhibit the activity of Hsp90.
US7041661 Use of thiazolobenzoheterocycles for treating multiple sclerosis The invention relates to the use of compound of Formula I in treating patients for inflammatory or neuropathic pain as well as various symptoms of multiple sclerosis
EP1328552A4 Crosslinked amide derivatives of hyaluronic acid and manufacturing method thereof The present invention relates to water-insoluble, crosslinked amide derivatives of hyaluronic acid and manufacturing method thereof, where the amide derivatives of hyaluronic acid are characterized by crosslinking, of polymer or oligomer having two or more amine groups, with hyaluronic acid or its hyaluronate salts through amidation reaction.The water-insoluble, crosslinked amide derivatives of hyaluronic acid according to the present invention may be diversely used for prevention of adhesion after surgical operation, correction of facial wrinkles, dermal augmentation, tissue engineering, osteoarthritic viscosupplement etc.
US20080227747 Composition and methods for treating or preventing degenerative joint and cardiovascular conditions A therapeutic composition and methods for the treatment and prevention of a degenerative joint disorder and/or a cardiovascular disease comprising polycosanols, glucosamine and chondroitin are disclosed.
CN102731291A Synthesis of 6-acetylenic acid compound and its application in antifungal field The invention discloses a synthesis technology capable of carrying out industrialization preparation of a 6-acetylenic acid compound and an application of the 6-acetylenic acid compound in antifungal medicines, and the synthesis technology comprises a salification reaction and an alkylation reaction.
CN103142535A Alginic sodium diester enteric tablet and preparation method thereof The invention discloses an alginic sodium diester enteric tablet and a preparation method thereof. The alginic sodium diester enteric tablet disclosed by the invention consists of an alginic sodium diester tablet core and an enteric coating layer coated outside the alginic sodium diester tablet core, wherein the alginic sodium diester tablet core comprises alginic sodium diester, filler and a disintegrant, and the enteric coating layer comprises an enteric material, a plasticizer, an antisticking agent and an opacifier; and during preparation, the alginic sodium diester enteric tablet is prepared through coating the enteric coating layer outside the alginic sodium diester tablet core. According the alginic sodium diester enteric tablet and the preparation method of the alginic sodium diester enteric tablet, the enteric effect is ideal, the bioavailability can be improved, and the stimulation to gastric mucosa caused by the drug is reduced; and the preparation method is simple, the quality of obtained products is stable, and thus, the method is applicable to large-scale production application.
WO2007110449A1 Benzenesulfonamide compounds and their use The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
EP2658859A2 Macrocyclic hepatitis c serine protease inhibitors The present invention relates to novel fluorinated macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.
CN101850105B Cefuroxime sodium composite medicine The invention provides a cefuroxime sodium composite medicine which is prepared from cefuroxime sodium, sodium glucuronate and glutathione in the weight proportion of 0.25-2.0:0.1-0.3:0.02-0.04. The invention also provides a preparation method of the composite medicine. The cefuroxime sodium composite medicine is superior to cefuroxime sodium prepared by the prior art in the aspects of safety, stability and curative effect.
US20110039916 Helper Virus-Free Herpesvirus Amplicon Particles and Uses Thereof The invention features new helper virus-free methods for making herpesvirus amplicon particles that can be used in immunotherapies, including those for treating any number of infectious diseases and cancers (including chronic lymphocytic leukemia, other cancers in which blood cells become malignant, lymphomas (e.g. Hodgkin's lymphoma or non-Hodgkin's type lymphomas). Described herein are methods of making helper virus-free HSV amplicon particles; cells that contain those particles (e.g., packaging cell lines or patients' cells, infected in vivo or ex vivo); particles produced according to those methods; and methods of treating a patient with an hf-HSV particle made according to those methods.
US8242146 Administering ROFLUMILAS and DICLOFENAC; antiinflammatory agents The invention relates to the combined use of a PDE4 inhibitor and a conventional NSAID in the treatment of an inflammatory disease and/or an inflammation-associated disorder while minimizing gastrointestinal side effects, such as gastric erosions and ulcer, which are frequently associated with the use of conventional NSAIDs. A preferred PDE 4 inhibitor for this combination is roflumilast or a derivative thereof. A preferred conventional NSAID for this combination is diclofenac or a derivative thereof.
CN103690516A Aripiprazole oral membrane and preparation method thereof The invention relates to an aripiprazole oral membrane and a preparation method thereof. The membrane is mainly prepared from 1-30% of aripiprazole, 30-80% of pullulan and additives. The membrane is rapid in disintegration and dissolution, is up to the accumulated dissolution rate of 85% at the moment of 5min, and can be completely dissolved out within 10min. The membrane is rapid in taking effects when used for treating schizophrenia and beneficial to the improvement of the compliance of patients suffering from mental disorders, and can be taken without chewing or water supplying.
CN1683339A 7-substituted-8-methoxy fluoroquinolone carboxylic derivatives, preparing process, preparation and use thereof The present invention relates to medicine chemistry and discloses 7-substituent-8-methoxy fluoro quinolone carboxylic derivative, i. e. 7-substituent-1-cyclopropyl-6-fluoro-1, 4-dihydro-8-methoxy-4-oxo-3-quinolone carboxylic acid and its salt; their preparation process and medicine composition for human and animal. The compounds of the present invention has antiseptic activity and safety higher than gatifloxacin and similar medicine.
CN102218064B Pharmaceutical combination with repaglinide and metformin as active components and preparation method thereof The invention relates to a pharmaceutical combination with repaglinide and metformin as active components and a preparation method thereof. The pharmaceutical combination comprises 0.1-10 weight portions of repaglinide and 100-1500 weight portions of metformin as active components and pharmaceutic adjuvants, wherein, the pharmaceutic adjuvants comprise filler, disintegrating agent, adhesive, flavoring agent, lubricant and swelling accessory, and the repaglinide is repaglinide crystal. The invention adopts the repaglinide crystal with small particle size, metformin and pharmaceutic adjuvants to prepare the pharmaceutical combination, so as to realize the purpose of simultaneous release. Since the particle size of the repaglinide used in the invention is small, the dissolvability is improved, so that the dissolution is improved and the bioavailability is increased.
US20100234377 Piperazine compounds for the inhibition of haematopoietic prostaglandin d synthase The present invention relates to compounds of general formula (I): wherein A, Y, X, n and B are as defined herein; and their use in the treatment and prevention of metabolic disorders, inflammatory conditions, allergic conditions, fever, pain including allodynia and nociception, eating disorders, cachexia, brain injuries, cancer of the genitals, sleep apnea, cardiovascular disease, flush effect associated with nicotinic acid and related compounds or for the promotion of wound healing. Certain compounds of general formula (I) are new and the invention also relates to these compounds and to their use in medicine.
WO2014106622A1 1,2,3-triazole-4-amine derivatives for the treatment of sigma receptor related diseases and disorders The present invention relates to new 1,2,3-triazole-amine derivatives of formula (I), having affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments for the treatment of sigma receptor related diseases and disorders.
WO2014124523A1 A method of treating obesity A method of treating obesity and obesity-related disorders in a mammal is provided. The method comprises the step of administering to the mammal a compound that inhibits the synthesis or activity of peripheral serotonin, including a Tph1 inhibitor or a serotonin receptor inhibitor.
CN101919855A Pharmacy application of piperazine ferulate The invention discloses pharmacy application of piperazine ferulate, and in particular application of piperazine ferulate and/or derivatives thereof to preparing drugs for preventing and/or treating pulmonary hypertension. The invention provides novel application of the piperazine ferulate and/or the derivatives thereof, i.e. application of the piperazine ferulate to preparing drugs for preventing and treating pulmonary hypertension, especially diseases with pulmonary vascular resistance progressive increase as main characteristic.
CN101015550A Preparing method of triptolide molecule microcapsule This invention relates to a method for preparing triptolide/beta-cyclodextrin inclusion compound, which is characterized in preparing according to the follow steps: (1) dissolving beta-cyclodextrin dissolve in double distilled water, placing in water bath with constant temperature, and making to beta-CD saturated solution; (2) dissolving triptolide in 1,2-propylene glycol, treating with ultrasound, adding beta-CD at a mol ratio of 1:2-4, heat dissolving with ultrasound, cooling for a night; and (3) placing on the millipore filter, air pump filtrating with Buchner funnel, washing with acetone, and drying to obtain white powdered form inclusion compound. The product of the invention can maintain the original property and efftect of triptolide, reduce local excitation and toxico-adverse side effect of triptolide, thereby improving pharmic security.
CN102716133A Application of quetiapine in preparation of medicines for preventing and treating autoimmune diseases The invention discloses an application of quetiapine in preparation of medicines for preventing and treating autoimmune diseases. Research results show that the quetiapine has an immune regulation function, can suppress proliferation of effector T cells, and alleviates infiltration of local lesion T cells. In an autoimmune disease model -- an experimental autoimmune encephalomyelitis model, administrating the quetiapine can prevent the paroxysm of animals in disease models, can relieve symptoms, shortens the duration of the symptoms, and acquires good therapeutic effects. According to the invention, not only the application range of the quetiapine is widened and the market value of the quetiapine is improved, but also a new way for preventing and treating the autoimmune diseases is provided.
CN101313980A Powder for removing acne, film for removing acne, beautifying liquid The invention relates to a composition of acne-dispelling ointment, an acne-dispelling mask and facial essence, a preparation method thereof and a matching use of the composition during the treating process. The preparation method comprises the following steps: Chinese violet, soirodela polyrhiza, oriental arborvitae, Salvia miltiorrhiza and radix scutellariae are alcohol extracted and concentrated and then prepared into the bubble oily ointment for standby; kushen, ageratum, capillary wormwood herb, herba agrimoniae, siberian cocklebcur herb and sibirian button bur are decocted, filtered and concentrated and then added with excipient to prepare the acne-dispelling mask for standby; calcined gypsum is ground into fine powder, added with subacid water at a temperature of 44 DEG C and stirred into the shape of paste, and then a gypsum mask is prepared; and 30 portions of radix sileris, 30 portions of angelica dahurica, 30 portions of green plum pulp, 30 portions of sweet chrysanthemum, 30 portions of snakegourd fruit and 30 portions of fruit almonds together with aloe facial cleanser are baked and ground into fine powder together, and then added with salicylic acid, sodium lauryl sulfate soap and acid water to prepare the facial essence for bottling and standby. The composition has the main efficacies of clearing away heat and toxic materials, activating blood circulation to dissipate blood stasis, and dispelling acnes and realizing facial beautification, and has obvious effects.
US20090130229 Antitumor uses of compound The use of an arylidene 2-indolinone derivative for treating tumors involving Met, PDGF-R, FGF-RI, FGF-R3 or Kit tyrosine kinases, or a Ret oncoprotein which includes a MEN2-associated mutation is disclosed.
US20120035176 Analogs of 3-o-acetyl-11-keto-beta-boswellic acid Analogs of 3-O-acetyl-11-keto-beta-boswellic acid and their method of preparation are presented. The analogs may be used as anti-inflammatory and anti-cancer agents. The compounds inhibit 5-lipoxygenase enzyme and various cell lines related to inflammation as well as to cancer showing a significantly better efficacy when compared to the normal boswellic acids. The analogs are capable of controlling and treating various inflammatory diseases and cancers.
CN103638075A Sesame oil suspension cream for scalds The invention provides sesame oil suspension cream for scalds. The sesame oil suspension cream for scalds is characterized by being formed by mixing and stirring calcium hydroxide aqueous liquor and sesame oil, which are of same parts by weight. The sesame oil suspension cream for scalds disclosed by the invention has the main characteristics that melting point is low, a medication method of the conventional ointment is improved, a defect that the conventional ointment contains a tannin component is overcome, the effects of promoting blood circulation to remove blood stasis, clearing away heat and toxic materials, wetting a wound surface, eliminating necrotic tissues and promoting granulation are improved; moreover, a preparation method of the sesame oil suspension cream for scalds is simple and convenient.
US20110098212 Cytokine A novel cytokine, U83A, is described, as are variant forms of the cytokine, having a wide range of agonistic and antagonistic activity against chemokine receptors. Uses of the chemokine in treatment of a range of diseases, including cancers and HIV/AIDS, are described.
US20130011426 Recombinant Vaccines and Use Thereof The present invention relates to fusion molecules of antigens, the nucleic acids coding therefor and the use of such fusion molecules and nucleic acids. In particular, said invention relates to fusion molecules, comprising an antigen and the trans-membrane region and cytoplasmic region of a MHC molecule and/or the cytoplasmic region of a MHC or a SNARE molecule.
EP1492798A1 N-(3-rifamycinyl)-carbamates, method of preparing them and their use for treating and preventing tuberculosis The present invention relates to novel N-(3-rifamycinyl)-derivatives, namely N-(3-rifamycinyl)-carbamates, methods of their preparation and their use for the production of pharmaceutical preparations. The invention also concerns a composition and a method for treating or preventing mycobacterial infections, especially tuberculosis. ____________________________________________
CN101919830A Novel application of 2,4-dimethoxyl trans-stilben The invention relates to novel application of 2,4-dimethoxyl trans-stilben, in particular to novel application of 2,4-dimethoxyl trans-stilben for cutting fat and resisting senile dementia.
US20110183926 Treatment using continuous low dose application of sugar analogs Methods and uses of low dosage nonmetabolizable D-glucose analogs and mannose analogs such as 2-deoxy-D-glucose, 5-thio-D-glucose, 2-fluoro-2-deoxy-D-glucose, 2-chloro-2-deoxy-D-glucose, 2-bromo-2-deoxy-D-glueose, 2-deoxy-2-fluoro-mannose, 2-deoxy-2-chloro-mannose, 3-deoxy mannose, 4-deoxy mannose, and 2,3 didioxy mannose, for the treatment of tumors.
WO2014111737A1 Composition for increasing of the effectiveness of uv-b therapy, process for the preparation thereof, and its use A light-therapeutic composition is disclosed, which can modify the optical characteristics of the skin, thereby increase the effectiveness of the UV-B therapy. The composition according to the invention includes one or more material, which sets the minimum value of wavelenght of the light transmitted, one or more material, which is suitable to modify the above-mentioned wavelenght value, and increase the transmittance of the skin in a certain wavelength-range, furthermore, optionally an excipient. The composition according to the invention blocks the UV radiation in the wavelength ranging from 280 to 300 nm, and helps the incorporation of the UV radiation by the skin in the wavelength ranging from 310 to 320 nm.˙
CN1839821A Cardiovascular pharmaceutical formulation, preparation method and uses Disclosed is a preparation for treating cardiovascular and cerebrovascular diseases, its preparing process and use, wherein the preparation comprises hippophe flavone, pharmaceutically acceptable inorganic bases and organic bases, or water-soluble inclusion compound formed from hippophe flavone and cyclodextrin, or low-molecular-weight alcohols, polysorbate, polyethylene glycol and poloxamer. The use of the hippophe flavone compound and preparation is also disclosed.
US20090239946 Pharmaceutical compositions of HDAC inhibitors and chelatable metal compounds, and metal-HDAC inhibitors chelate complexes The present invention provides pharmaceutical compositions of an HDAC inhibitor and a chelatable metal compound. In one embodiment, the invention provides a method of treating cancer and alleviating the side effects of the HDAC inhibitor by administering the pharmaceutical composition. In another embodiment, the present invention also provides pharmaceutical compositions of metal HDAC inhibitor chelate complexes. In another embodiment, the invention provides methods of treating cancer by administering the pharmaceutical compositions. The invention provides crystalline compositions of metal HDAC inhibitor chelate complexes and methods of producing same.
EP1503989A1 Dopamine receptor modulators as antipsychotic agents The invention provides compounds of formula (I):wherein A and B represent the groups -(CH2)m- and -(CH2)n-respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, -(CH2)pC3-6cycloalkyl, -(CH2)pOC3-6cycloalkyl, -COC1-6alkyl, -SO2C1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -CO2C1-6alkyl, -CO2NR7R8, -SO2NR7R8, -(CH2)pNR7R8, -(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R3 represents hydrogen or C1-6alkyl; R4 represents optionally substituted aryl or optionally substituted heteroaryl; R5 and R6 each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, -(CH2)pC3-6cycloalkyl, -(CH2)pOC3-6cycloalkyl, -COC1-6alkyl, -SO2C1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -CO2C1-6alkyl, -CO2NR7R8, -SO2NR7R8, -(CH2)pNR7R8, -(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R7 and R8 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; and either: Z represents -CR9R10X- or -XCR9R10- and X represents oxygen, sulfur, -SO- or -SO2, or Z represents -CONR11- or -NR9CO- and X represents -CH2-, oxygen, sulfur, -SO- or -SO2; R9 and R10 each independently represent hydrogen, C1-6alkyl or fluoro; R11 represents hydrogen or C1-6alkyl;or a pharmaceutically acceptable salt or solvate thereof.The compounds of the invention are useful in therapy, in particular as antipsychotic agents.
CN102584828A Pyrrolidine[3,4-d]pyrimidine derivative and preparation method and application thereof The invention discloses a pyrrolidine[3,4-d]pyrimidine derivative and a preparation method and an application thereof. The pyrrolidine[3,4-d]pyrimidine derivative is an inhibitor of a type I insulin-like growth factor receptor (IGF-1R), and has a good IGF-1R inhibiting function and a good cancer cell proliferation inhibiting function, so that the pyrrolidine[3,4-d]pyrimidine derivative can be taken as a therapeutic agent for treating tumors and relevant diseases.
CN103110665A Composition for maintaining genital tract micro-ecological barrier and application thereof The invention discloses a composition for promoting formation of a genital tract micro-ecological barrier and balancing the balance and application thereof. The composition is characterized in that proliferation of effective microbial community in the genital tract can be stimulated, and proliferation in the genital tract or proliferation of the passing pathogenic bacteria is not stimulated. The composition comprises the following components in percentage by mass-volume: 5-20 percent of oligosaccharide, 5-10 percent of probiotics metabolite, 0.2-20 percent of water-soluble pharmaceutical adjunct and the balance of deionized water. The invention also discloses a method for preparing the composition, as well as application in condoms, lubricating agents and related articles so as to exert the biological action.
US7638508 Glucocorticosteroid compound having anti-inflammatory activity A compound of formula (I): wherein X represents O or S; R1 represents C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkylmethyl or C3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R1 represents aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 represents hydrogen, methyl, which may be in either the α or β configuration, or methylene; R3 and R4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond; or a physiologically acceptable salt or solvate thereof, and pharmaceutical formulations and methods of use thereof.
US20100028346 Novel synergistic effects The present invention encompasses a combination of at least one conjugate and one or more chemotherapeutic agent(s) which when administered exerts an unexpectedly enhanced therapeutic effect. The therapeutic effectiveness of the combination is greater than that of the conjugate alone or the administration of one or more of the drug(s) without the conjugate. The present invention is also directed to compositions comprising at least one conjugate and at one or more of chemotherapeutic agent and to methods of treating cancer using at least one conjugate and at least one or more of chemotherapeutic agent (s). The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of one or more chemotherapeutic agent(s) and at least one conjugate. In each case, such combination has therapeutic synergy or improves the therapeutic index in the treatment of cancer over the anticancer agent(s) alone.
CN103690521A Calcium zinc gluconate oral solution The invention relates to a medicinal preparation composition, and in particular relates to a calcium zinc gluconate oral solution. The composition comprises the following components: calcium gluconate, zinc gluconate, lysine hydrochloride, lactic acid, aspartame, acesulfame, sodium chloride, sodium benzoate, essence, sodium hydroxide and purified water.
WO2009123588A1 Amides of 3, 5-substituted-is0xaz0le-4-carb0xylic acids for the treatment of viral infections, cancer and restenosis The invention is directed to the use of compounds of Formula I as anti-viral agents, anti-cancer agents and agents for inhibiting restenosis: NR2R3 The variables in Formula (I) are defined herein.
US20120058087 Diagnosis of endometritis The present invention relates to methods for diagnosing and treatment of a dormant infection of at least one pathogen. The invention further relates to a composition comprising an anti-dormancy factor as well as to said composition for use in a method of diagnosis or treatment and also to a method for manufacturing said composition. The invention further relates to a kit of parts comprising, inter alia, said composition. The invention also relates to a method for activating a dormant infection.
US20100227828 New synergistic phytochemical composition for the treatment of obesity Synergistic anti-adipogenic and pro-lipolytic compositions for the prevention and amelioration of adipogenesis and lipolysis mediated diseases, comprising at least two extracts selected from enriched demethylated curcuminoids obtained from Curcuma longa, Moringa oleifera and Murraya koenigii. The anti-adipogenic and pro-lipolytic compositions optionally contain one or more anti-obesic agents. These compositions are useful for preventing anti-inflammatory and free radical mediated diseases.
US20110268749 Treatment of cancer via targeting of il-13 receptor-alpha2 Disclosed herein are compositions and methods for treating or preventing cancer involving the use of a TNF-alpha antagonist, an IL-13Rα2 antagonist, and/or a AP-I antagonist.
CN103554188A 6-(azacyclo-substitute) anthraquinone platinous chloride complex as well as preparation method and application thereof The invention discloses a 6-(azacyclo-substitute) anthraquinone platinous chloride complex as well as a preparation method and an application thereof. The 6-(azacyclo-substitute) anthraquinone platinous chloride complex disclosed by the invention has the structure of a formula I. The complex disclosed by the invention has good anti-tumor activity and security, and has great application values in treating lung cancer, liver cancer, leukemia, colon cancer and ovarian cancer in the medicine field.
EP1423117B1 2-substituted 1-arylpiperazines as tachykinin antagonists and/or serotonin reuptake inhibitors The present invention relates to piperazine derivatives of formula (I), wherein R represents halogen, C1-4 alkyl, trifluoromethoxy or trifluoromethyl; R1 is trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, halogen or trifluoromethoxy; R2 is hydrogen, C1-4alkyl or C2-6alkenyl; R3 represents hydrogen or C1-4alkyl; n and m are independently 0 or an integer from 1 to 3; and pharmaceutically acceptable salts and solvates thereof, process for their preparation and their use in the treatment of condition mediated by tachykinins and/or by selective inhibition of the serotonin reuptake transporter protein.
US20050214385 Chromium/biotin treatment of dyslipidemia and diet-induced post prandial hyperglycemia A method for treating dyslipidemia and/or post prandial hyperglycemia by administering a combination of a chromium complex and biotin to an individual in need thereof is disclosed. The two compounds are administered orally or parenterally in daily dosages which provide between 25 μg and 1,000 μg of chromium and between 25 μg and 20 mg biotin. A method for reducing the glycemic index of food is similarly provided.
US20080008770 contains calcium; dietetics A composition for reducing the weight of a human. The composition is provided in the form of a capsule comprising an effective amount of capsaicin and/or analogs thereof, L-tyrosine, supplemental caffeine and/or and analogs thereof, green tea extract containing catechin and caffeine, and embodiments which include calcium. The invention is also directed toward methods for reducing and maintaining weight of a human using the composition.
CN102697770A Murraya paniculata leaf and application of mono compound in preparation of sedative and hypnotic drugs The invention relates to the field of medicine and discloses a Murraya paniculata leaf, a Murraya paniculata leaf extractive and new biological activity of part of a flavonoid mono compound extracted from Murraya paniculata leaves, namely discloses a Murraya paniculata leaf, a Murraya paniculata leaf extractive and the use of part of a flavonoid mono compound extracted from Murraya paniculata leaves in preparation of sedative and hypnotic drugs, anxiolytic drugs, anticonvulsive drugs or antimanic drugs, in particular to the use in preparation of sedative and hypnotic drugs.
CN102600112A Film agent dispersing or dissolving in oral cavity and utilizing fentanyl as main medicine active agent A film agent dispersing or dissolving in an oral cavity and utilizing tentanyl as a main medicine active agent can disperse or dissolve in the oral cavity, is taken conveniently, takes effect quickly, and is convenient to carry, good in taste and particularly suitable for being taken by old people and children.
CN102218056A Use of butenolide I in preparing drugs for controlling immunological liver injury The invention discloses a use of butenolide I for preparing drugs for controlling immunological liver injury. With the present invention, the butenolide I can reduce levels of TNF-alpha and NO, wherein the TNF-alpha and the NO play important roles in a pathogenic process of the immunological liver injury; the butenolide I can reduce elevated levels of the NO and the iNOS in liver homogenates of immunological liver injury mice so as to decrease the liver injury induced by the NO; the butenolide I can inhibit a overexpression of the TNF-alpha so as to decrease the direct liver injury or the indirect liver injury induced by the TNF-alpha. In addition, the use of the butenolide I as the drug for controlling the immunological liver injury has advantages of convenient preparation, extensive sources, low price and high safety, and has good development and application prospect.
US7319102 Pyrrolo[2,3-d]pyrimidine cytokine inhibitors The present invention relates to 2,6,7-substituted pyrrolo[2,3-d]pyrimidines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 2,6,7-substituted pyrrolo[2,3-d]pyrimidines and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.
CN101961418A Double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch The invention discloses a double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch. The patch is divided into an upper layer and a lower layer; a medicament on the upper layer is one or more of menthol, peppermint oil, borneol and a non-steroidal anti-inflammatory medicine which has synergy with capsaicin and can dispel or alleviate local discomfort reaction to the capsaicin, particularly penetrates into the skin more rapidly than the capsaicin to respond, has synergetic therapeutic effect with the capsaicin, and can dispel or alleviate local discomforts such as burning sensation and the like in the initial usage period of the capsaicin; the capsaicin on the lower layer of the patch exists in the form of a cyclodextrin inclusion compound; the patch fully absorbs water after being used on the skin for 6 to 8 hours; and the capsaicin is slowly released from the inclusion compound and penetrates into the skin. The double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch overcomes the defects of short tolerance time and poor medication compliance of a patient during the transdermal administration of high-dosage capsaicin, and facilitates achieving the maximum pharmacological effect of a medicament.
US20120109051 Devices, methods, and kits for taste modification and controlling food intake Disclosed are various embodiments of intra-oral taste modification devices, both erodible and non-erodible, and methods for using the devices, and methods and kits for making the devices, for controlling food intake by reducing the desire to eat highly sweetened foods and refined carbohydrates.
US20090156619 Heterocycle Substituted Amide and Sulfur Amide Derivatives as Histone Deacetylase (HDAC) Inhibitors The present invention related to compounds of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Compounds of the present invention are useful for treating or preventing neurodegenerative diseases, schizophrenia and stroke among other diseases.
US7387994 Antitumor, anticancer agents; particles or coils or stents coated solid-phase agent comprising a binding agent comprising collagen are directed to target vasculature, such as the vasculature of solid tumor masses or aneurysms The present invention relates generally to methods and compositions for targeting and delivering solid-phase platelet-dependent vascular occlusion agents. In particular, particles or coils or stents coated with platelet binding agents are directed to target vasculature, such as the vasculature of solid tumor masses or AV-malformations or aneurysms or endoleaks; the solid-phase agent then binds and activates platelets, which in turn bind and activate other platelets. This process results in the rapid formation of a platelet-mediated thrombus about the solid-phase agent causing vessel occlusion.
US20120082728 Multifunctional stealth nanoparticules for biomedical use The present invention relates to the field of drug delivery nanosystems. More precisely, the present invention concerns a copolymer with advantageous properties for the outer coating of various nanoparticles. Said copolymer comprises at least three types of monomers with stealthy, coupling and therapeutic properties respectively, as well as an optional fourth type of monomers with targeting properties. The present invention also relates to core-shell or hollow shell nanoparticles coated by an external layer of the copolymer according to the invention. Several types of core-shell nanoparticles are envisaged. The invention also concerns methods for preparing said nanoparticles, as well as pharmaceutical compositions or medicaments comprising them.
US7361666 Ligands for cellular receptors, including opiate receptors; side effect reduction; base structure is a saturated nitrogen-containing ring substituted with a tertiary amide that is N-substituted with an arylalkyl group One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
CN101732310A Application of epothilone B The invention relates to application of epothilone B in preparing a medicament for treating Gleevec medicament resistant chronic myelogenous leukemia.
US20110319491 Anhydrous depigmenting compositions comprising, within the fatty phase thereof, a solubilized phenolic compound and a retinoid Novel anhydrous dermatological depigmenting compositions, especially for topical application, contain, within the fatty phase thereof, as pharmaceutical active agents, a dissolved phenolic compound and a retinoid.
US7425641 Carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof, the prodrugs and the salts thereof which have valuable properties. The compounds of the above general formula I wherein R5 denotes a cyano group are valuable intermediate products for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein R5 denotes one of the amidino groups mentioned in claim 1 have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.
CA2371857C Gardos channel antagonists Novel inhibitors of potassium flux are disclosed. The inhibitors show surprising resistance to degradation in biological media and enhanced in vivo half-lives relative to non-fluorine substituted homologues. Methods for the use of these compounds include treating sickle cell disease, preventing erythrocyte dehydration and inhibiting potassium flux.
US20110171232 Methods of treating autoimmune diseases caused by small intestinal bacterial overgrowth Disclosed is a method of diagnosing autoimmune diseases, such as multiple sclerosis and systemic lupus erythematosus, which involves detecting the presence of small intestinal bacterial overgrowth (SIBO) in a human subject having at least one symptom associated with a suspected diagnosis an autoimmune disease. Also disclosed is a method of treating these autoimmune diseases, which involves at least partially eradicating a SIBO condition in the human subject. The method includes administration of antimicrobial or probiotic agents, or normalizing intestinal motility by employing a prokinetic agent. Also disclosed is a kit for the diagnosis or treatment of autoimmune diseases.
US20120288533 Protein-polysaccharide conjugates and use for encapsulating nutraceuticals for clear beverage applications The present invention provides protein (or peptide)-polysaccharide (or oligosaccharide) conjugates (PPC) as nanocapsular vehicles for nanoencapsulation of biologically active compounds, particularly nutraceuticals. The PPCs efficiently protect both hydrophobic (i.e., water insoluble) and hydrophilic (i.e., water soluble) nutraceuticals, to provide a composition which, when added to a beverage, disperses so as to provide a clear or transparent solution. In some embodiments, the PPCs are Maillard reaction based PPCs. Advantageously, the conjugates of the present invention protect the nutraceuticals from degradation, both during shelf life and upon gastric digestion.
WO2008035686A1 Agent for improving insulin resistance Disclosed is an agent for improving the insulin resistance or a therapeutic agent for type-II diabetes, which is safe and highly effective. Specifically disclosed is an agent for improving the insulin resistance or a therapeutic agent for type-II diabetes, which comprises a compound represented by the general formula (I) or a salt thereof as an active ingredient. (I) wherein R1, R2 and R3 independently represent a lower alkyl, a lower alkenyl, a lower alkynyl, an aralkyl, an araryl, a phenyl or a hydrogen atom.
WO2007049626A1 Oral solid preparation containing cabergoline An oral solid preparation which is an oral solid preparation containing cabergoline having good storage stability, characterized in that it contains a) cabergoline as an active ingredient, b) a sugar and/or a sugar alcohol, and c) a hydrophobic substance, and is prepared without using a solvent or without substantially bringing cabergoline into contact with a solvent. The oral solid preparation of the invention can be produced by dry mixing or dry granulation of a) cabergoline, b) a sugar and/or a sugar alcohol, and c) a hydrophobic substance.
WO2007003741A3 Polyphenol type compounds, compositions containing same and use thereof for preventing or treating diseases involving abnormal cell proliferation The invention concerns compounds of formula (I), wherein- XmR1 and YnR2, identical or different are present, or one of the XmR1 or YnR2 is absent and YnR2, identical or different, is present, and in that case the bond between C1 and C2 is a double bond, XmR1 and YnR2 together represent a group A and in that case the bond between C1 and A is a double bond, or their pharmaceutically acceptable salts as medicine.
US20050159611 Process for producing shogaols and intermediates for the synthesis thereof In accordance with the invention, an industrial process for producing shogaols useful in the fields of for example foods, flavor, pharmaceutical products, qui-pharmaceutical products and cosmetics can be provided. The invention relates to novel intermediates represented by the following general formula and a process for producing shogaols from the intermediates. In accordance with the invention, shogaols can readily be produced, of which mass production has been difficult because shogaols have been produced only by the extraction process from a natural ginger. Intermediates; (in the formula (1), R1 represents hydrogen atom or methyl group; R2 represents optionally branched alkyl group with one to 18 carbon atoms; R3 and R4 each independently represents hydrogen atom, a lower alkyl group or a protective group of the phenolic hydroxyl group; A represents an alkylene group with one to 4 carbon atoms; and X represents benzenesulfonyl group or toluenesulfonyl group.)
WO2008131348A3 Compositions and methods for treatment of uncontrolled cell growth Compositions and methods are provided for the treatment of cancer and other diseases of uncontrolled cell growth. Inhibitors of t-RNA and 28s rRNA are provided as are non-functional amino acid residues for charging of t-RNA molecules. Therapeutic application of the above inhibitors is also provided for the treatment of cancer.
US7514107 Treatment of diseases involving defective gap junctional communication This invention relates to compositions containing polyphenols, for example, cocoa polyphenols such as flavanols and their related oligomers, and methods for treating abnormalities in gap junctional communication of cells, such as cancer, heart arrhythmia, neuro-degenerative diseases and cognitive dysfunction.
CN101548943A Inhalation nebulizer containing formoterol The invention relates to a solution containing formoterol. When the solution is used, the content is released out in a mist state under various pressures of a hand pump, an ultrasonic nebulizer, an air compressor, and the like, and is used for pulmonary medicament inhalation delivery.
CN101195616A Compound with antineoplastic activity, production method and application thereof The invention relates to a thistle longipeduncle kadsura lactone compound as formula (I) and a thistle lactone compound as formula (II), wherein in the formula (I), R1, R2, R3, R4, R5, R6 are -H, -OH, -OCH3 or -OCOCH3, or R1 and R2, R3, R4, R5 and R6 are formed with double bonds or three-membered epoxies, or R1 and R5, R2 and R4 are formed with oxygen bridges, R7, R8, R9 and R10 are -H, -OH, -OCH3 or -OCOCH3, or R7 and R8, R9 and R10 are formed with double bonds, or R9 and R10 are formed with three-membered epoxy, in the formula (II), R1, R2, R3, R4, R5 and R6 are -H, -OH, -OCH3 or -OCOCH3, or R1 and R2, R3 and R4, R5 and R6 are formed with double bonds or three-membered expoy, or R1and R5, R2 and R4 are formed with oxygen bridges, R7, R8, R9, R10 and R11 are -H, -OH, -OCH3 or -OCOCH3, or R7, R8, R9 and R10 are formed with double bonds.
CN103690479A Glycopyrronium bromide injection and preparation method thereof The invention discloses glycopyrronium bromide injection and a preparation method thereof. The preparation method disclosed by the invention comprises the following steps of: (1), adding 50-90% of injection water into a preparation tank, adding sodium chloride, adding a pH adjusting agent after dissolving to adjust the pH value to 1.0-4.0, and then, diluting to total weight by adding injection water to obtain solution A; (2), adding glycopyrronium bromide into the solution A at the constant temperature of 30-40 DEG C, stirring till dissolving completely, crudely filtering in a filtrate tank through a milliporous filtration membrane which is 0.45 mu m, and finally filtering through a milliporous filtration membrane which is 0.22 mu m to obtain an intermediate product; (3), filling the filtrate tank into a neutral boron-silicon container, sealing, and sterilizing through steam at 115-121 DEG C for 8-30 min to obtain the glycopyrronium bromide injection. The glycopyrronium bromide injection disclosed by the invention has the characteristics of being good in stability, high in safety and the like.
WO2014048869A1 Substituted indazol-pyrrolopyrimidines useful in the treatment of hyperproliferative diseases The present invention relates to substituted indazol-pyrrolopyrimidine compounds of general formula (I):in which R1a, R1b, R1c, R1d, R2a and R2b are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
US20090069363 Therapeutic Agent for Constipation A therapeutic and/or prophylactic agent for constipation induced by a compound having an opioid μ receptor agonist activity, which agent comprises as an effective ingredient a compound having an opioid δ receptor antagonist activity, e.g., a compound of Formula (I): (wherein R1 represents hydrogen, lower alkyl, cycloalkyl lower alkyl or the like; R2 and R3 independently represent hydrogen, hydroxy or the like; R4 is hydrogen, hydroxy or the like; R5 is hydrogen; R4 and R5 may optionally form —O— or the like; R6 represents hydrogen, lower alkyl or the like (wherein X represents —O— or —N(R10)— or the like; R7, R8, R9a and R9b independently represent hydrogen, lower alkyl, lower alkoxycarbonyl or the like; r represents an integer of 0 to 5; Y represents —CH— or the like; Z represents a crosslinkage composed of 2 to 5 atoms) or a pharmaceutically acceptable salt thereof or a solvate of either.
CA2405238C Single-dose antihistamine/decongestant formulations for treating rhinitis An oral once-per-day single dosage unit for treating the symptoms of rhinitis formulated with a nasal decongestant having a duration of action of not more than about sixteen hours and antihistamine. Preferably, the antihistamine is non-sedating.
CN103169709A Application of thiadiazolo pyrimidone compounds in treatment of hypercalcemia and tumor bone metastases The invention relates to an application of thiadiazolo pyrimidone compounds with a structural general formula (1) in treatment of hypercalcemia and tumor bone metastases. The compounds are PTH (parathyroid hormone) receptor antagonists, and the variables in the structural general formula (1) are as defined in the specification.
WO2008053136A1 2-(hetero-)aryl,4-carbonyl substituted pyrazole derivatives as inhibitors of p38 mitogen-activated protein kinase Compounds of formula (I) are inhibitors of p38 MAP kinase activity, and are useful in the treatment of, inter alia, inflammatory and autoimmune disease wherein Ring A is aryl, heteroaryl or heterocyclyl of 5-13 atoms; Ring B is optionally substituted aryl or heteroaryl of 5-13 atoms; Z is (a) a radical of formula -(CH2)z-X1-L1-Y- NHCHR1R2 or (b) a radical of formula -(CH2)z-Y1-L1-R wherein R1R2CHNH- and R are respectively N- and C-linked amino acid or amino acid ester groups as defined in the description, and -Y-L1-X1-(CH2)z- and -L1-Y1-(CH2)z- are linker radicals as defined in the description; R7 is hydrogen or -C(=O)R' where R' is hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl or (C1-C6)haloalkyl; R8 is hydrogen or (C1C6)alkyl; R9 is hydrogen, halogen, hydroxyl, (C1-C6)alkoxy, (C1-C6)alkyl; R18 is hydrogen, halogen, hydroxyl, (C1C6)alkoxy (C1-C6)alkyl, - NRaRb where Ra and Rb are hydrogen or (C1-C6)alkyl, or optionally substituted aryl, heteroaryl or heterocyclyl or Ra and Rb when taken together with the nitrogen to which they are attached form a cyclic amino group of up to 6 ring atoms; R19 is hydrogen, halogen, (C1C6)alkoxy, or (C1C6)alkyl.
CA2243824C Therapeutic agent for keratoconjunctiva diseases The present invention provides a novel substance which promotes the production and secretion of mucin in ophthalmic tissues. The therapeutic agent for keratoconjunctiva diseases according to the present invention contains gefarnate as an active ingredient. This therapeutic agent for keratoconjunctiva diseases is applicable to dry eye, keratitis, conjunctivitis, corneal erosion, corneal ulcer, etc. The dosage form is preferably an ophthalmic solution.Concentration of gefarnate is, for example, 0.1-3% (w/v).
CA2390746C Quinolinone derivative pharmaceutical composition and production method therefor A quinolinone derivative pharmaceutical composition comprising a quinolinone derivative represented by the structural formula (I): (see formula I) wherein the quinolinone derivative is in the form of particles, which have an average particle diameter of 0.5 to µm and such a particle size distribution that particles having a particle diameter of 15 µm or less account for 90% or more of the totality of the particles, and also have a fusion enthalpy of 30 J/g or more, and the surface of the particles are coated with a water-soluble composition containing a water-soluble polymer, can quickly dissolve an active ingredient in the digestive tract and is also superior in long-term storage stability.
WO2008114008A1 9-substituted-8-oxo-adenine compounds as toll-like receptor (tlr7 ) modulators The present invention provides compounds of formula (I): wherein R1, Y1, X1, L and R2 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use as modulation of toll-like receptor (especially TLR7).
CA2673005A1 Emulsions comprising non-esterified phytosterols in the aqueous phase The present invention provides a stable emulsion in which: a) an aqueous phase comprises one or more phytosterols or phytostanols, or mixtures thereof in free (non-esterified) form; and b) an oil or fat phase comprises phytosterols or phytostanols, or mixtures thereof, in esterified form. The invention further provides foods, beverages, nutraceuticals and pharmaceuticals of which the unique emulsion of the present invention forms all or part, useful in the treatment or prevention of cardiovascular disease and its underlying conditions.
CA2678069A1 Derivatives and analogs of chroman as functionally selective alpha2c adrenoreceptor agonists In its many embodiments, the present invention provides a novel class of chroman compounds of formula I as .alpha.2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of prepaxing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the .alpha.2C adrenergic receptors using such compounds or pharmaceutical compositions.
US7524857 Pharmaceutical combinations based on pyridoindolone derivatives and anticancer agents The invention relates to the combination of compounds of formula: with one or more anticancer agents.
US20100099767 Topical Pharmaceutical Formulation A composition for topical application of an NSAID comprises a solution or suspension of the NSAID in a carrier system comprising a polyhydric alcohol, a glycol ether and an ester of A higher fatty acid, the carrier system being present as a single phase at ambient temperatures. The NSAID may be diclofenac as diclofenac acid. The polyhydric alcohol may be a glycol such as isopropylene glycol and the glycol ether may be a diethylene glycol ether such as diethylene glycol monoethyl ether.
US7045529 Imidazopyrimidinyl and imidazopyri dinyl derivatives Provided herein are compounds of the formula (I): as well as stereoisomers and pharmaceutically acceptable salts thereof. Such compounds are, because of their ability to antagonize CRF, useful in the treatment of a variety of disorders characterized by execssive CRF expression. These include, for example: affective disorder, anxiety, depression, headache, irritable bowel syndrome, post-traumatic stress disorder, supranuclear palsy, immune suppression, Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, gastrointestinal diseases, anorexia nervosa or other feeding disorder, drug addiction, drug or alcohol withdrawal symptoms, inflammatory diseases, cardiovascular or heart-related diseases, fertility problems, human immunodeficiency virus infections, hemorrhagic stress, obesity, infertility, head and spinal cord traumas, epilepsy, stroke, ulcers, amyotrophic lateral sclerosis and hypoglycemia.
CN101780043B Preparation method of sanguinarine liposome with acid sensitivity The invention relates to the field of pharmaceutical preparation, in particular to a preparation method of sanguinarine liposome with acid sensitivity, which is characterized by selecting citric acid ammonium salt for preparing the sanguinarine liposome when an ammonium salt gradient method is adopted for preparation. The sanguinarine liposome prepared by the method of the invention has acid sensitivity and is favorable to the antitumor effect.
US20090042960 1-Cycloalkyl-5-Iodotetrazoles The compounds of the formula (I) in which R1 represents cycloalkyl, and its stereoisomers and any mixtures thereof are highly suitable as microbicides for protecting plants and materials.
EP1140965B1 Antibacterial protonated oligonucleotides The novel discovery that protonated nucleic acids inhibit bacterial growth is reported and methods for the preparation and therapeutic use of nuclease resistant and acid resistant protonated/acidified nucleic acids for administration to animals including man, to treat or prevent a bacterial infection are described.
US20100056581 Substituted Piperidino Phenyloxazolidinones The present invention relates to certain substituted piperidino phenyloxazolidinones. Specifically, the invention relates to geminally disubstituted piperidino phenyloxazolidinones having antimicrobial activity with improved pharmacokinetic profile. The invention also relates to processes for the preparation of compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods for treating or preventing microbial infections using the compounds of the present invention.
US20080241255 Enhanced inhalation delivery to lungs; effective for wide range of medicants The disclosure relates to a method of enhancing nicotine or other medicament concentrations in a gaseous carrier. The methods are adaptable to the delivery of nicotine or other medicaments for therapeutic effect in various diseases, in particular nicotine for tobacco product use cessation, substitution and/or harm reduction. The disclosure further relates various devices and device design principles for practicing these methods.
US20110033537 Sustained Drug Release Composition The invention relates to a sustained release formulation for delivering one or more pharmaceutically active agents. The formulation comprises cross-linked high amylose starch and at least one pharmaceutically active agent, and optionally can be subdivided into smaller dosage forms where the smaller dosage forms have substantially the same sustained release properties as the formulation from which they were derived. The formulations can provide sustained release for up to at least 24 hours, and because of their divisability permits a recipient of the active agent or the person administering the active agent to titrate the dosage of the agent.
WO2010092485A2 Combined treatment of multiple sclerosis The invention concerns a novel treatment multiple sclerosis, based on induced anaemia, followed by administration of an erythropoiesis-stimulating agent (ESA). In a preferred embodiment, the ESA is darbopoietin alpha, CERA or Hematide. The anaemia is induced by successive bloodlettings or by administration of an iron chelator, such as deferiprone, deferoxamine, polyanionic amines, substituted polyaza compounds, desferrithiocon, hydroxybenzyl-ethylenediamine-diacetic acid and pyridoxal isonicotinoyl hydra z one.
US20070105868 3-(2-{5-methyl-2-[4-(trifluoromethyl)piperidin-1-yl]-1,3-thiazol-4-yl}ethoxy)phenyl]acetic acid,peroxime proliferator-activated receptor antagonists; side effect reduction; very low toxicity, especially hepatotoxicity; metabolic disorders; antidiabetic agents; anticholesterol agents; antilipemic agents The present invention relates to the compound represented by formula (I) (wherein R1 and R2 is hydrogen atom, C1-8 alkyl etc.; R3 is C1-8 alkyl which may be substituted with 1 to 3 halogen atom(s), phenyl; R4 is hydrogen atom etc.; R5 and R6 is hydrogen atom, C1-8 alkyl etc.; X is sulfur atom or oxygen atom etc.; ringA is cyclic group which may have a substituent(s).), or a salt thereof. Toxicity of the compound represented by formula (I) is very low, and it is safe enough to use as a pharmaceutical agent and since it has PPAR δ agonistic activity, it is useful as preventive and/or therapeutic agent for glucose.lipid metabolic disorder, hypertension, circulatory diseases etc.
WO2005013964A1 Pharmaceutical preparation containing nateglinide A pharmaceutical preparation which contains nateglinide in an amount of at least 26 wt.% based on the whole preparation and contains at least one disintegrator selected among carmellose or a salt thereof, sodium carboxymethyl starch, croscarmellose sodium, crospovidone, partially gelatinized starch, and hydroxypropyl cellulose having a low degree of substitution in an amount of at least 28 wt.% based on the whole preparation. The preparation has a high nateglinide content and the nateglinide is rapidly absorbed to reduce blood sugar. The preparation is small and is easy to take.
CN101543471A Rumen glucose The invention relates to rumen glucose, which is a rumen particle prepared from glucose by a microcapsule enveloping technique so that the glucose is not degraded in the rumen and is effectively released in intestinal canals. The enveloped substance not only can effectively treat bovine ketosis, but also can effectively prevent ketoses, and can provide rumen carbohydrates for cattle to improve the milk yield at the same time.
CN101548945A Long-acting flunixin meglumine injection and method for preparing same The present invention relates to a long-acting flunixin meglumine injection for animals and method for preparing same. The invention provided flunixin meglumine injection delays medicine absorption so as to prolong medicine action time by adding proper polyvinylpyrrolidone and poloxamer high molecular compound in the preparation process. Approved by clinical experiments that action time of the invention is longer than common flunixin meglumine injection, the invention reduces labor strength and reduces stress response of animals with more obvious medicine effect, and capable of using with long-acting antibacterials to provide a synergistic effect. The invention provides a animals specific medicine of long-acting, effective antipyretic, antiphlogosis and analgesic for veterinary clinical.
CA2451626C One dose vaccination with mycoplasma hyopneumoniae The present invention relates to methods for treating or preventing a disease or disorder in an animal caused by infection by Mycoplasma hyopneumoniae (M. hyo) by administering to the animal at approximately three (3) to ten (10) days of age, a single dose of an effective amount of a M. hyo vaccine. The M. hyo vaccine can be a whole or partial cell inactivated or modified live preparation, a subunit vaccine, or a nucleic acid or DNA vaccine. The M. hyo vaccine administered in accordance with the present invention can be synthesized or recombinantly produced.
CN103494803A New application of dehydrated andrographolide The invention provides the application of dehydrated andrographolide in preparing medicine used for suppressing diseases caused by tumor cells related to the activity of ANO1 ion channel proteins. The dehydrated andrographolide can selectively suppress the activity of the ANO1 ion channel proteins on the tumor cells, therefore, the proliferation, the metastasis and the invasion of the tumor cells can be blocked, and a new idea for treating tumors can be provided by applying the dehydrated andrographolide to the preparation of tumor depressants.
US20080009445 Anti-endotoxic, antimicrobial cationic peptides, the encoding DNA and methods of use thereof A novel class of cationic peptides having antimicrobial activity is provided. Exemplary peptides of the invention include KWKSFIKKLTSAAKKVVTTAKPLALIS (SEQ ID NO:3) and KGWGSFFKKAAHVGKHVGKAALTHYL (SEQ ID NO:15). Also provided are methods for inhibiting the growth of bacteria utilizing the peptides of the invention. Such methods are useful for the treatment of respiratory infections, such as in cystic fibrosis patients. Such methods are further useful for accelerating wound healing.
CN103130806A Phenanthroindo(quio)lizidine alkaloid derivative, and preparation, anti-TMV activity, anti-HIV activity and anti-tumor activity thereof The invention relates to a phenanthroindo(quio)lizidine alkaloid derivative I, and a preparation, anti-tobacco mosaic virus (TMV) activity, anti-human immunodeficiency virus (HIV) activity and anti-tumor activity thereof. A general formula I has very good anti-plant virus activity, can well inhibit the tobacco mosaic virus and has very good anti-human immunodeficiency virus (HIV) activity and anti-tumor activity. In the formula, specific representation contents of substituents n, X, Y and R1-R5 are defined in the specification.
EP1844781A1 Use of sodium channel blockers for the treatment of preterm labor The present invention refers to the use of sodium channel blockers such as tetrodotoxin or saxitoxin, its analogues/derivatives as well as their acceptable salts, for the production of a medicament for the treatment of preterm labor and/or premature birth.
CN103110612A Tetrandrine dry powder inhalant and preparation method thereof The invention discloses a tetrandrine dry powder inhalant and a preparation method thereof. The preparation method comprises the following steps of: spraying and drying tetrandrine and tetrandrine organic acid saline liquor formed by an organic acid; collecting the obtained micropowder; and physically mixing with a lactose carrier to form the tetrandrine dry powder inhalant, wherein the distribution range of particle size of lactose carrier is 1-300 microns, and the organic acid is selected from citric acid, tartaric acid or malic acid. According to the invention, the tetrandrine is prepared as the dry powder inhalant which is combined with radiotherapeutic medicines to treat lung caner to realize the targeting purpose, and is directly used to treat the focus. The bioavailability is improved, the first-pass effect is avoided, and the compliance of patients is improved by way of inhalation to deliver.
EP2245006B1 Sulfonamides as orexin antagonists The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3 and n are as described in the description and claims. The compounds are orexin receptor antagonists may be useful in the treatment of disorders, in which orexin pathways are involved.
EP2275535A1 Animal cells and processes for the replication of influenza viruses Animal cells are described which can be infected by influenza viruses and which are adapted to growth in suspension in serum-free medium. Processes for the replication of influenza viruses in cell culture using these cells are furthermore described, as well as vaccines which contain the influenza viruses obtainable by the process or constituents thereof.
CN103120720A Convergent and divergent agent and preparation method thereof The invention relates to a convergent and divergent agent which is prepared from medical lime and rheum officinale and is mainly used to treat skin trauma of patients with diabetes and other suppulative refractory wounds.
CN103450115A Curcumin derivative and application of curcumin derivative as cannabinoid receptor modulator The invention relates to the preparation of a curcumin derivative and application of the curcumin derivative as a cannabinoid receptor modulator. In the synthetic route of the curcumin derivative, 10% of Pd-C is used for reducing the curcumin; for protecting a phenolic hydroxyl group, only 2.0% mol of DMAP (Dimethylaminopyridine) is used for catalysis and (Boc)2O of which the mole amount is 2.05 times as much as that of the curcumin is used so that reaction is completely realized; during a Mannich reaction, Mannich reagents such as N,N,N',N'-tetramethyldiaminomethane prepared in advance are used so as to avoid that an acid component reacts with formaldehyde to generate by-products at first. In the whole route, the target compound is obtained through reducing, protection, alkylation, deprotection and the Mannich reaction with the curcumin as the raw material. The route has the characteristics of cheap and available raw material, high yield and easy operation. The curcumin derivative is capable of inhibiting the hepatic stellate cells of a hepatic fibrosis rat from synthesizing and secreting extracellular matrix through a cannabinoid receptor, promoting the degradation of the extracellular matrix, reducing the deposition of the extracellular matrix in the liver and further developing the effect of treating the hepatic fibrosis.
US20080181939 hydrolysis triggered, controlled release polymersome nano-system for delivering a cytotoxic, anticancer therapeutic active agent to cell; stable, synthetic, self-assembling, controlled release, polyethylene oxide-based vesicles; semi-permeable, thin-walled, amphiphilic, high molecular weight Provided are methods for preparing and delivering stable, purely synthetic, self-assembling, controlled release, polyethylene oxide (PEO)-based polymersome vesicles, and the resulting PEO-based polymersomes capable of such controlled release, and methods of use therefor for the controlled transport and delivery of encapsulatable, cytotoxic, anticancer active agents contained therein. Further provided are methods for controlling destabilization of the vesicle membrane and the resulting hydrolysis-triggered, controlled release of active agent(s) encapsulated in the vesicle by controlling the blend ratio (mol %) of hydrolysable PEO-block copolymer of the hydrophilic component(s) and of the more hydrophobic PEO-block copolymer component(s) to produce amphiphilic high molecular weight PEO-based polymersomes, wherein the PEO volume fraction (fEO) and chain chemistry control encapsulant release kinetics from the copolymer vesicles and the polymersome carrier membrane destabilization.
CN102357222A Muscle-relaxing blood-invigorating pain-relieving paste and preparation method thereof The invention discloses formulation and a preparation method of a muscle-relaxing blood-invigorating paste for treating diseases such as cervical spondylosis, scapulohumeral periarthritis, lumbar disc herniation, sciatica, systemic soft tissue injury, calcaneus pain, gout, periostitis, fracture convalescence, and the like.
CN103637995A Vitamin C tablets and preparation method The invention provides vitamin C tablets and a preparation method. By changing the accessory formula in the original production technology, the stability of the vitamin C tablets is effectively improved, and the quality problem that the vitamin C tablets easily change color in a storage process is solved. In the production technology, the accessories include 30-60% of dextrin, 1-5% of starch, 10-20% of carboxymethyl starch sodium, 1-5% of hydroxypropyl methylcellulose, 10-30% of microcrystalline cellulose, 1-5% of tartaric acid and the balance of lubricant, wherein the lubricant is 30-70% of ethanol. The vitamin C tablets provided by the invention have smooth surfaces and stable performance and are suitable for mass production; the quality of the products meets the requirements of the Chinese pharmacopoeia.
EP1910345A1 Substituted amides, their preparation and their use as pharmaceuticals The present invention provides new substituted amides of the general formula (I) in which D, L, M, W and B are as defined in the description, their tautomers, their enantiomers, their diastereomers, mixtures thereof and salts thereof, particularly their physiologically acceptable salts with organic or inorganic acids or bases, which have valuable properties. The compounds act as inhibitors of factor Xa.
CA2746922A1 Compositions and methods for increasing lean muscle mass after exercise The present invention relates to novel methods and compositions comprising casein, creatine or derivatives of creatine, branched chain amino acids and proteases useful for increasing lean muscle mass after exercise.
EP1962822A1 Therapy of malignant neoplasias The present invention provides a 3-iodo-L-phenylalanine or 4-iodo-L-phenylalanine for the preparation of a pharmaceutical composition for the treatment of malignant neoplasia. Moreover, the invention provides a method for the treatment of malignant neoplasia, the method comprising the steps of administering 3-iodo-L-phenylalanine or 4-iodo-L-phenylalanine to a subject in need thereof and a pharmaceutical composition comprising 3-iodo-L-phenylalanine or 4-iodo-L-phenylalanine.
WO2014151567A1 Oral care compositions containing deoxy sugar antimetabolites Described herein are oral care compositions comprising a deoxy sugar antimetabolite and methods of inhibiting microbial biofilm formation and/or degrading a microbial biofilm in a subject.
CN101792375A Sesquiterpene compound in tobacco stems and preparation method and application thereof The invention relates to a novel sesquiterpene compound (A) and a preparation method and application thereof. The preparation method comprises the following steps: tobacco stem samples are extracted by ultrasonic with dichloromethane three times after being crushed; an extracting solution is concentrated into an extract; the extract is primarily separated by silica gel column chromatography, and is further separated by semipreparative high performance liquid chromatography to obtain the required novel compound. The in vitro antibacterium and antitumor activity screening of the compound is carried out, and the experiment result shows that the compound of the invention has stronger antibacterium and antitumor activity.
US7449450 Compounds, methods of screening, and in vitro and in vivo uses involving anti-apoptotic genes and anti-apoptotic gene products Novel polypeptides having anti-apoptotic activity, and methods of screening for such novel polypeptides having anti-apoptotic activity, and polynucleotides encoding such polypeptides; Compounds that regulate or modulate apoptosis and/or anti-apoptotic activity, such as compounds having anti-apoptotic activity, and such as compounds that induce, restore, or modulate apoptosis and/or inhibit, diminish, or modulate anti-apoptotic activity, methods of screening for such compounds, and methods of using such compounds in the therapeutic treatment of diseases; Methods of treating eukaryotic cells with compounds that regulate or modulate apoptosis and/or anti-apoptotic activity; Methods of enhancing the stability, growth, and/or productivity of eukaryotic cells; Pharmaceutical compositions that regulate or modulate apoptosis and/or anti-apoptotic activity.
CN102327278A Application of carborane derivatives, nano compound preparation and application of nano compound preparation The invention provides carborane derivatives and application thereof. The structural formulas of three relative novel carborane derivatives are shown as (1), (2) and (3), and antibacterial medicines used as active ingredients of a medicine have the effects of resisting clinically common pathogenic bacteria (staphylococcus aureus, acinetobacter baumannii, klebsiella pneumonia, and proteus mirabilis), and also have the same-degree effect of resisting multidrug-resistant staphylococcus aureus strains and can inhibit multidrug resistance of the multidrug-resistant staphylococcus aureus strains, wherein a compound (2) can react with medicine-resistant staphylococcus aureus extracellular proteins, so adhesion of bacteria on the surface of an organism is reduced, and the formation of a medicine-resistant strain biological film is inhibited. The toxicity and invasiveness of staphylococcus aureus are reduced, treatment efficiency is improved, an adverse effect caused by using a large amount ofantibiotics is avoided, and a novel compound is provided for finding a novel medicine for resisting medicine resistance bacteria.
WO2007126060A1 Salt of 1,2-dihydropyridine compound Disclosed is an acid addition salt of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one or a hydrate of the acid addition salt, wherein the acid used in the acid addition salt is selected from the group consisting of benzenesulfonic acid, p-toluenesulfonic acid, hydrochloric acid, hydrobromic acid, sulfuric acid, methanesulfonic acid, fumaric acid, tartaric acid, succinic acid, and benzoic acid.
DE102009016719A1 Composition, useful as pharmaceutical preparation for e.g. prophylaxis of lipid metabolic disorders in humans and animals and treating atherosclerosis, comprises 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor and solid material Composition comprises: (a) at least one 3-hydroxy-3-methylglutaryl-co enzyme A reductase inhibitor; and (b) a solid material, which is obtained by drying a liquid aqueous formulation comprising (i) a vesicular structured coenzyme Q 1 0and/or its derivatives (1-60 wt.%), (ii) lecithin and/or its derivatives (0.1-30 wt.%) and (iii) a vesicle stabilizer (5-90 wt.%) of at least one polyol (s) consisting of aldose, ketose, reduced aldose, reduced ketose, glycoside of aldose, glycoside of ketose, 4-6C-tri-, tetra-, penta-, hexaol or maltodextrin. - ACTIVITY : Antiarteriosclerotic; Muscular-Gen; Antilipemic. - MECHANISM OF ACTION : 3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor. The ability of the composition to inhibit HMG-CoA reductase was tested in 2 male subjects by administering simvastatin (20 mg) with the freeze-dried nanoscale vesicular structured high bioavailability coenzyme Q 1 0(60 mg) for 6 weeks followed by a 2 week washout period. The result showed that the coenzyme Q 1 0plasma level was 1.71+- 0.62 after 6 weeks as compared to the coenzyme Q 1 0plasma level of 1.21+- 0.51, which was observed after 30 minutes.
EP2264171A1 Anti-myosine Va siRNA and skin depigmentation Isolated small interference RNA (siRNA) comprising a sense RNA strand and a complementary anti-sense RNA strand forming together a RNA duplex, where the sense RNA strand comprises a sequence, which has a distinct nucleotide in comparison to a fragment of 14-30 contiguous nucleotides of the exon F nucleotide sequence of the myosin Va protein coding gene, is new. An independent claim is included for a composition comprising the siRNA and a support. - ACTIVITY : Dermatological. - MECHANISM OF ACTION : Melanogenesis inhibitor.
CN101693014A Process for preparing coenzyme A medicament freeze drying preparation The invention discloses a process for preparing a coenzyme A medicament freeze drying preparation, which comprises steps of preparing medical liquor, removing bacteria, filtering, filling and freeze drying, wherein the freeze drying step includes pre-freezing, primary drying and secondary drying. The invention shortens freezing time from more than 20 hours to hours between 13 and 16, reduces 20%-35% of energy consumption, simultaneously improves 20%-35% of production capacity under the circumstance of no increase of hardware investment owing to shortened freeze drying time, thereby saving energy, increasing production and greatly lowering production cost.
CN103467258A Lignanoid compound, and preparation method and use thereof The invention provides a lignanoid compound having a structure represented by formula (I), and also provides an application of the compound in the preparation of medicines for preventing or treating cancers. The compound has a novel structure and a good antitumor activity. The formula (I) is shown in the specification.
CN1623540A Unit dose form cantharide acid freeze-dried powder injection preparation and its preparation method A freeze-dried powder injection of cantharidic acid for treating tumor is prepared from the cantharidic acid or its pharmacolgoically acceptable salt, and at least one pharmacologically acceptable carrier chosen from excipient, pH regulator, antioxidizing agent and stabilizer. Its advantages are high curative effect and high stability.
CN102078375A Externally-used medicine for diminishing inflammation, swelling subsidence and relieving pains on surface of wound The invention discloses an externally-used medicine for diminishing inflammation, swelling subsidence and relieving pains on a surface of a wound, which can quickly heal the surface of the wound. The technical solution of the externally-used medicine comprises the following components: lamiophlomis rotata, polyethylene glycol 400, double-bond quaternary ammonium salt, menthol crystal and emulsion accessories.
WO2014159248A1 Tricyclic compounds as inhibitors of immunosuppression mediated by tryptophan metabolization Presently provided are inhibitors of IDO and TDO and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase and tryptophan 2,3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
WO2006038041A1 Besylate salts of six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain The present invention provides a compound of formula I: Y-J-NH-Z (I) 10 wherein: Y is a quinoline or isoquinoline optionally substituted wit h one or two substituents independently chosen from hydroxy, halogen, haloC1-4 alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two 15 substituents in dependently chosen from hydroxy, halogen, haloC1-4alkyl, C1-4alkyl, C3-5cycloalkyl, C1-4alkoxy, hydroxyC1-4alkyl, cyano, hydroxy, C1-4cycloalkoxy, C1-4alkylthio, haloC1-4alkoxy, nitro, Q, (CH2)p Q, -NR2R3 , -(CH2)pNR2R3 and -O(CH2)pNR2R3; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted with one or two substituents independently selected 20 from halogen, haloC1-4alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; Q is phenyl, a five-membered heterocyclic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, or a six-membered heterocyclic ring containing one, two or three nitrogen atoms, optionally substituted by C1-4alky l; each R2 and R3 is chosen from H and C1-4alkyl, or R2 and R3 , together with the nitrogen atom to 25 which they are attached, may form a six-membered ring optionally containing an oxygen atom or a further nitrogen atom, which ring is optionally substituted by C1-4alkyl or Q; p is 1, 2 or 3; as the besylate salt; pharmaceutical compositions comprising it; its use in methods of therapy; use of it for manufacturing medicaments; and methods of using it to treat diseases requiring administration of 30 a VR1 antagonist such as pain, cough, GERD and depression.
WO2009000087A1 Substituted fused pyrimidines as antagonists of gpr105 activity Fused pyrimidine compounds of structural formula (I) are effective as antagonists of the biological activity of the GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and Metabolic Syndrome.
CN101259125B Anethol trithione injection emulsion and preparation thereof The invention relates to an anethol trithione injectable emulsion and a preparation method thereof. The major proposal of the invention is that: an oil phase and a water phase is respectively heated, a medicine is added into the oil phase, then the oil phase is added into the water phase (or the water phase is added into the oil phase) and stirred into a rough emulsion, the PH value of the rough emulsion is adjusted, homogenized by an autogizer, and sterilized, and the product is prepared. Anethol trithione has definite curative effects on choleretic function, liver protection, ptyalize, detoxification, digestion promoting, etc., and can significantly strengthen the vitality of liver cells, enhance the secretion of bile, cholalic acid, and bile pigment and intensify the detoxifying function of liver, and can be used for treating cholecystitis, cholelithiasis, acute and chronic hepatitis and hepatocirrhosis, etc. The anethol trithion of the invention can provide a safer, more effectiveand more convenient injection, thus greatly enhancing the bioavailability of the medicine.
CN103255061A Penicillium griseofulvum, antibacterial active compound generated thereby and application The invention provides a?Penicillium griseofulvum?CPCC400528, the preservation number of which is CGMCC NO.5752. The Penicillium griseofulvum CPCC400528 can be fermented to generate an antibacterial active compound with a molecular formula of C7H6O4 and a structure shown as formula (I). The compound has a good growth inhibition effect on a variety of Gram positive pathogenic bacteria and Gram negative pathogenic bacteria. With the increase of concentration, the inhibition effect is gradually enhanced. Also, the compound has a good inhibition effect on a plurality of drug resistant strains. The Penicillium griseofulvum strain provided in the invention is easy to ferment and culture and has a high yield. The preparation process of the active compound is simple and is easy to control. The prepared compound has obvious antibacterial activity, lays the foundation for research and development of new antibacterial drugs, and has very broad market prospects.
CN102247335A Bufalin dry powder inhalant as well as preparation method and application thereof The invention relates to a dry powder inhalant, in particular to a Bufalin dry powder inhalant, the preparation method of the dry powder inhalant and the application in preparing drug for treating lung tumors. The Bufalin dry powder inhalant is characterized in that the Bufalin dry powder inhalant is composed of Bufalin and pharmaceutically acceptable auxiliary materials, wherein the mass ratio of the Bufalin to pharmaceutically acceptable auxiliary materials is (1:0.01)-(1:110). The dry powder inhalant by taking the Bufalin as the main drug can directly act on an affected part by aiming at the lung tumor to lower the possibility of toxic and side effect and improve the bioavailability. According to the Bufalin dry powder inhalant, the defects that the oral-administration preparation slowly takes effect, the preparation has low bioavailability and the like can be overcome, and the problems of low Bufalin content, inconvenient use, poor patient complicance and the like in the injectioncan be solved. Thus, the Bufalin is prepared into the dry powder inhalant, which has great prospect for developing new drug.
CN102716113A Pharmaceutical composition comprising curzerene The invention belongs to the technical field of medicines and provides a pharmaceutical composition comprising curzerene. The pharmaceutical composition also comprises germacrone, furanodiene, curdione, beta-elemene, curcumol and borneol besides the curzerene. The components of the pharmaceutical composition are definite, and the quality can be controlled. The weight part of the curzerene is controlled, thus the irritation of the medicine is reduced. The pharmaceutical composition can be used for preparing suppositories, ointments, capsules, effervescent tablets, gels, lotions and film or foam agents. The pharmaceutical composition has a good effect of treating HR-HPV (high risk human papillomavirus) and/or LR-HPV (low risk human papillomavirus) infection and other diseases and can be used widely clinically.
WO2006052889A2 Quinolinone-carboxamide compounds The invention provides novel quinoline-carboxamide 5-HT4 receptor agonist compounds of the formula (I). The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
WO2006022344A1 Utilization of anti-mortalin 2 antibody and functional nucleic acid in treating cancer A treatment for cancer with the use of an antibody binding to mortalin 2 and a functional nucleic acid. Mortalin shows upregulated expression in immortalized cells or tumor tissues. Immortalized human cells with overexpression of mortalin show scaffold-independent proliferation. By injecting K antibody that is a specific anti-mortalin antibody into a tumor of a nude mouse, the tumor growth is regulated or the tumor size is reduced compared with a control. Namely, it is intended to provide the utilization of a specific anti-mortalin antibody (K antibody) in treating tumor and utilization thereof as a carrier molecule for transporting an immunotoxin or the like into cells. It is indicated that mortalin serves as a target in treating cancer. Thus, a novel and efficacious anticancer agent is provided. Moreover, an anti-mortalin antibody internalized in cells is developed and various methods of using the same are provided.
EP2696863A1 Use of calixarenes associated with an antibiotic in the treatment of bacterial infections The invention relates to a product comprising at least one given antibiotic and a calixarene for use as a drug.
US7556948 Method for producing crystallized pleuromutilins Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.
US7208521 Selective inhibitors of the urokinase plasminogen activator The present invention relates to novel selective inhibitors of the urokinase plasminogene activator (uPA, EC3,4.21.31) of the aryl guanidine type.
US20110257266 Therapeutic Regimen and Methods for Treating or Ameliorating Visual Disorders Associated Disclosed herein are therapeutic regimens for treating or ameliorating a visual disorder associate with an endogenous retinoid deficiency in a subject by administering a therapeutically effective amount of a synthetic retinal derivative or a pharmaceutically acceptable composition comprising a synthetic retinal derivative according to the therapeutic regimen which leads to local recovery of visual functions such as visual fields, visual acuity and retinal sensitivity, among others.
US20100069449 Novel oxazolidinone derivative with difluorophenyl moiety, pharmaceutically acceptable salt thereof, preparation method thereof and antibiotic composition containing the same as an active ingredient Novel oxazolidinone derivatives with a difluorophenyl moiety, represented by Chemical Formula 1, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same as an active ingredient are provided. Exhibiting potent inhibitory activity against Gram-positive bacteria including Haemophilus influenza and Coagulase negative staphylococci and resistant bacteria including vancomycin-resistant enterococci (VRE), the pharmaceutical composition is useful as an antibiotic. (wherein, R is as defined in the specification)
EP1931349A2 Use of sodium channel blockers for the management of musculoskeletal pain The invention provides methods for managing musculoskeletal pain. The compounds useful in the methods of the invention are blockers of sodium ion channels, and in particular compounds that bind to the SSl or SS2 extracellular mouth of the a- subunit thereof. Particularly useful compounds are saxitoxin and its derivatives and analogues and tetrodotoxin and its derivatives and analogues.
US20120071449 Pharmaceutical composition for inhalation The present invention relates to a pharmaceutical composition for inhalation. The invention is further directed to a method for setting the performance characteristics of such a pharmaceutical composition and the use of such a composition in the treatment of asthma, COPD, allergies, infectious diseases and diseases of the cardiovascular system.
EP1968574B9 Use of benzo-fused heterocycle sulfamide derivatives for the treatment of obesity The present invention is a method for the treatment of obesity, for promoting weight loss and / or suppressing appetite comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) as herein defined.
US7022694 Indoles and indolines having 5-HT activity The present invention provides compounds of Formula (I): wherein R1, R2, R3, R4, R5, R6 and --- have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are useful as 5-HT ligands.
EP1731155A2 Beta-D-2', 3' -Didehydro-2',3' -Dideoxy-5-Fluorocydine for use in the treatment of HIV infections The present invention discloses a method for treating HIV that includes administering β-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using β-D-D4FC as "salvage therapy" to patients which exhibit drug resistance to other anti-HIV agents. β-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.
CN101205218A Substituted cinnamyl piperazine as well as preparation and uses thereof The invention provides a replaced cinnamon piperazine derivative and medicine salt or solvate, which comprises the following general structure: R1, R2 and R3 are same to or different from each other and the hydrogen, nitro, hydroxy, halogen, saturaged or unsaturated alkyl or alkoxy containing 1 to 8 carbons and alkyla containing 1 to 8 carbons are selected. The replaced cinnamic acid is coupled with the 3, 4-dichloro 1-benzyl-piperazine through the dicyclohexyl carbodiimide so as to prepare and obtain the compound of the invention. The invention has strongly effective cytotoxic activity over a plurality of tumor cells and can be applied in the preparation of the medicines for controlling the tumor diseases.
WO2009009951A1 2'-fluoro-4'-substituted nucleosides, the preparation and use 2'-Fluoro-4'-substituted nucleosides analogues, their prodrugs and 5'-phosphates, their preparation and use. The compounds have the general formula: wherein . . The said compounds are used in the synthesis of medicine used for treating viral infection, especially HBV, HCV, HIV infection.
US20120165305 Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.
CN103705890A Pharmaceutical composition with function of removing heat from lung to relieve cough The invention discloses a medicament with a function of removing heat from lung to relieve cough. The medicament is prepared from the following raw materials in parts by weight: 60-100 parts ephedra, 140-180 parts of gypsum, 120-160 parts of semen armeniacae amarae, 30-50 parts of sessile stemona root, 30-50 parts of tussilago farfara, 30-50 parts of thunberg fritillary bulb, 60-100 parts of white mulberry root bark, 60-100 parts of cordate houttuynia, 60-100 parts of Chinese mahonia stem, 18-30 parts of pericarpium citri reticulatae, 30-50 parts of liquorice, 60-120 parts of fresh momordica grosvenori and 5-15 parts of fresh ginger. The medicament is clinically used for dispelling wind and opening the inhibited lung-energy, relieving cough and reducing sputum, and is suitable for improving symptoms of cough, expectoration and the like.
WO2011044978A1 Sulfoxide derivatives for treating tumors The invention relates to sulfoxide derivatives of the formula Ia to Im as described and to the pharmaceutically usable salts, solvates, enantiomers, tautomers, and stereoisomers thereof, including mixtures thereof in all ratios for treating tumors.
EP1545453B1 Rifalazil for treating infections of clostridium difficile The invention features methods and compositions including rifalazil for treating Clostridium difficile.
US6956052 treatment of cancer and inflammation-associated disorders, such as arthritis; for example,1-[4-(aminosulfonyl)phenyl]-8-{[(trifluoromethyl)sulfonyl]amino}-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
US20100273726 Methicillin-resistant staphylococcus aureus active metabolites isolated from laurus nobilis and combinations thereof This present provides kaempferol-3-(2-E,3-Z-di-p-coumaroyl)-rhamnoside, kaempferol-3-(2-Z-3-E-di-p-coumaroyl)-rhamnoside, and kaempferol-3-(2,3-di-Z-p-coumaroyl)-rhamnoside compounds useful as a new class of anti-bacterial agents. These compounds are extracted from Platanus occidentalis or Laurus nobilis. These compounds were found to exhibit anti-bacterial activity against methicillin resistant Staphylococcus aureus (MRSA).
CN1823817A Electrolyte nutrition fortification agent An electrolyte as nutrient intensifier for preventing the function disorder and hyporesistance caused by absence of electrolyte in human body contains K, Na, Ca, Mg and vitamins.
CN102657866A Cancer prevention and fighting capsules The invention belongs to a high-end functional health care food, and discloses hard capsules which are prepared from the following raw materials: natural plant component garlicin, isothiocyanate, curcumin, ellagic acid, resveratrol, immunoglobulin (fungus polysaccharide), shark cartilage, coumarin, superoxide dismutase, glutathione, lycopene and selenium-enriched yeast. The capsules have effects of cancer prevention and fighting, auxiliary inhibition of tumor, rehabilitation and chemoradiotherapy after tumor operation, enhancement of killing power of the tumor by a medicament and the like. A manufacturing process of the product comprises the following steps of: mixing the raw materials; mixing; filling capsules; performing pass test; and packaging into a formal product.
CN103239404A Dual-targeted liposome, and preparation method and application thereof The invention discloses a dual-targeted liposome, and a preparation method and application thereof. The dual-targeted liposome comprises liposome and ligands for surface modification, wherein the ligands are folic acid and transferrin. The invention also provides a preparation method of the dual-targeted liposome, and application of the dual-targeted liposome in preparation of a drug for treating brain glioma. The dual-targeted liposome disclosed by the invention is modified by two ligands, plays the dual-targeted role, and can help doxorubicin hydrochloride span a blood brain barrier; and transferrin and folic acid of the dual-targeted liposome disclosed by the invention are safe and nontoxic, are inherent ingredients in the body, and are high in security and good in biocompatibility.
US20050226870 Administering anti-inflammatory amount of a purified antibody specific against C5, wherein antibody inhibits the cleavage of C5 into C5a and C5b The use of compounds that block complement component C5 or its active fragments C5a and/or C5b (such compounds collectively referred to as “C5 blockers”) to treat established joint inflammation (arthritis) is disclosed. Administration of such C5 blockers has been found to: 1) arrest and/or reduce inflammation in joints which are already inflamed, and 2) inhibit the spread of inflammation to unaffected joints.
CA2341642C Page-4, an x-linked gage-like gene expressed in normal and neoplastic prostate, testis and uterus, and uses therefor PAGE-4 is a gene preferentially expressed in normal male and female reproductive tissues, prostate, testis, fallopian tube, uterus and placenta, as well as in prostate cancer, testicular cancer and uterine cancer. This expression pattern makes it a target for diagnosis and for vaccine based therapy of neoplasms of prostate, testis and uterus. The invention provides immunogenic compositions comprising PAGE-4 protein or immunogenic peptides thereof, methods of inhibiting the growth of malignant cells expressing PAGE-4, and methods of inducing an enhanced immune response to PAGE-4-expressing cancers.
EP1611888A1 Antitussives An antitussive which comprises, as an active ingredient, a tricyclic compound represented by Formula (I) [wherein R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like, X1-X2-X3 represents CR5=CR6-CR7=CR8 (wherein R5, R6, R7 and R8 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like, Y represents -CH2S- or the like, and R2 represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like] or a pharmaceutically acceptable salt thereof.
US20110002944 Compositions and Methods to Promote Neural Cell Growth The instant invention provides methods and compositions for promoting neural cell growth by inhibiting myelin associated glycoprotein (MAG)-induced inhibition of axonal regeneration. The invention relates to methods for identifying agents that inhibit MAG-induced inhibition of neural cell growth. Methods for inhibiting myelin associated glycoprotein (MAG)-induced inhibition of neural cell growth in a patient, methods for treating or preventing a MAG-induced disease or disorder of the CNS or PNS, comprising the step of administering at least one of the compositions according to this invention are provided. The invention includes kits comprising one or more agents identified according to the invention.
CN102964459A Lentinan calcium complex, and preparation method and application thereof The invention provides a lentinan calcium complex, and a preparation method and application thereof. The method comprises the steps of: adding a calcium chloride solution to an aqueous solution of lentinan with stirring, at 40-80 DEG C, regulating a pH value to 7-10 with sodium hydroxide, and continuously stirring for 1 h for a complex reaction; removing free calcium ions by a dialysis method; and concentrating and freeze-drying the lentinan compound solution to obtain the lentinan calcium complex with calcium content of 5.2mg / g. Compared with a blank group, the lentinan calcium complex can obviously promote mouse macrophage RAW264.7 to release immune factors, such as a tumor necrosis factor TNF-alpha and a cell factor IL-6. The preparation method of the lentinan calcium complex provided by the invention is simple and easy for practice. Besides, as an organic calcium, the lentinan calcium complex can also promote calcium absorption and improve immunity.
WO2006125181A3 Piperidine derivatives and their use as stearoyl-coa desaturase modulators Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where p, G, J, L, M, W, R2, R3, R4 and R5 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
WO2014057995A1 Extract and formulation including extract The objective of the present invention is to provide an extract from inflamed rabbit skin inoculated with vaccinia virus and formulations, etc. including the extract which have greater uniformity in quality. By using the amount of N-acetyl neuraminic acid contained in the extract from inflamed rabbit skin inoculated with vaccinia virus and the formulations including the extract as an index, greater uniformity of the extract and the formulations can be ensured for each production lot. The extract from inflamed rabbit skin inoculated with vaccinia virus and the formulations including the extract, which are produced in this manner so as to have greater uniformity, are extremely useful with effectiveness and safety more rigorously secured.
US20110086069 Pharmaceutical formulations of nitrite and uses thereof The present invention relates to pharmaceutical compositions of nitrites such as inorganic nitrites, or any pharmaceutically acceptable salts, solvates, or prodrugs thereof, and the medical use of these compositions. The pharmaceutical compositions, which can be formulated for oral administration, can provide immediate release or extended release of the nitrite ion (NO2 −). The pharmaceutical compositions of the invention are useful, for example, for the treatment of chronic tissue ischemia.
CN103282495A Novel anti-dr5 antibody The present invention relates to an antibody which has a therapeutic effect on cancer, autoimmune diseases or inflammatory diseases. Namely, the present invention relates to an antibody which exhibits an apoptosis-mediated cytotoxic activity on a cell expressing a death domain-containing receptor. The present invention addresses the problem of providing a drug which has a therapeutic effect on cancer. The present invention clarifies that a novel anti-DR5 antibody, which is capable of inducing apoptosis in a cell, has a remarkable cytotoxic activity compared with the conventional anti-DR5 antibodies.
WO2013152717A1 Fused pyrimidine compound, and preparation method, intermediate, composition， and uses thereof Disclosed are a fused pyrimidine compound as represented by formula (I), pharmaceutically acceptable salt, hydrate, and solvate thereof, an optical isomer or a prodrug thereof, as well as a preparation method, an intermediate, a composition and uses thereof. The fused pyrimidine compound according to the present invention can inhibit activity of PI3 kinase, and can be used to treat diseases such as cancer caused by abnormal activity of the PI3 kinase, or can be used to prepare medicine for treating these diseases.
US20100151066 Composition for suppressing appetite, improving tone and mood, with a natural antidepressant activity and with an antiasthenic effect Compositions comprising L-tryptophan, 5-hydroxytryptophan and/or D-Limonene are used for preparing a product suitable for sublingual or nasal administration which is helpful in suppressing appetite in such a manner as to promote weight loss in an individual; such compositions furthermore exhibit an antidepressant activity and an antiasthenic effect which makes them helpful in improving tone and mood and the level of attention in an individual. The compositions preferably comprise phenylethylamine in a synergistic combination which substance is contained in an algal plant extract, preferably of Klamath algae.
WO2013169989A1 Method and compounds for inhibiting the mcm complex and their application in cancer treatment A method for treating cancer by using an agent which is capable of inhibiting the functionality of the MCM complex, a heterohexameric ring formed from six subunits, in the process of DNA replication and a method of screening for such agents by detecting the locations and functions of the MCM subunits, such as hMcm2 and hMcm6, in cells treated with candidate compounds.
WO2009060209A1 6,6-fused bicyclic aromatic compounds and their therapeuti use This invention relates to a class of 6,6-fused bicyclic aromatic compounds which are ligands of the CRTH2 receptor (Chemoattractant Receptor-homologous molecule expressed on T Helper cells type 2), and their use in the treatment of diseases responsive to modulation of CRTH2 receptor activity, principally diseases having a sgnificant inflammatory component. the invention also relates to novel members of that class of ligands and pharmaceutical compositions containing them.
US6846827 Antiinflammatory agents; antiallergens; antiarthritic agents The invention concerns pyrimidine derivatives of Formula (I) wherein m is 0-3 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R3 is hydrogen, halogeno or (1-6C)alkyl; n is 0-2 and each R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; p is 0-4; and Q1 is aryl or heteroaryl; or pharmaceutically acceptable salts or in vivo cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
CN102961384A Medical application of przewaquinone A The invention discloses application of przewaquinone A, namely a diterpenoid quinine compound, in preparation of a medicament for resisting tumor vessel angiogenesis. According to the invention, the przewaquinone A is taken as an angiogenesis inhibitor and a malignant tumor resisting reagent, wherein the angiogenesis inhibitor can be used for inhibiting proliferation and diffusion of malignant cells by inhibiting angiogenesis in malignant tissues. Experiments prove that the przewaquinone A can be used for effectively inhibiting the proliferation of the malignant cells and has an obvious inhibition effect on the abnormal growth of the vessels, and therefore the przewaquinone A can be used for preparing the medicament for resisting the tumor vessel angiogenesis.
CN102727722A Topical hemostatic powder The invention, pertaining to a field of medical technology, relates to a topical hemostatic powder. The topical hemostatic powder is prepared by the following powdered materials by weight: 10 to 15 parts of male woodlouse, 13 to 20 parts of bile arisaema, 13 to 20 parts of blood scorpion, 20 to 28 parts of myrrh, 2 to 5 parts of fried nux vomica, 7 to 10 parts of keel, 7 to 10 parts of angelica, 12 to 18 parts of safflower, 7 to 10 parts of kawa, 7 to 12 parts of crab bone, 25 to 35 parts of pure frankincense, 13 to 17 parts of divaricate saposhnikovia root, 20 to 28 parts of cibotiumbarometz, 6 to 11 parts of pseudo-ginseng, 12 to 17 parts of dahurian angelica root, 7 to 10 parts of flagleaf, 10 to 14 parts of ligusticum chuanxiong hort, 7 to 12 parts of borneol, 11 to 17 parts of cimicifuga foetida and 11 to 18 parts of paris polyphylla. The topical hemostatic powder of the invention has the advantages of good analgesic and hemostatic effects, notable curative effect, simple preparation process, convenient storage, taking and using and can be used for hemostasis, analgesia and detumescence of a traumatic injury, an operation and the like.
CN102960309A Minipig chronic pulmonary hypertension animal model and construction method thereof The invention discloses a minipig chronic pulmonary hypertension animal model. A monocrotaline solution is injected to an abdominal cavity of a male or female healthy minipig which is 1-5 months old and is 3-15kg in weight; and the minipig chronic pulmonary hypertension animal model is obtained after the monocrotaline solution is injected for 4-9 weeks. Correspondingly, the invention discloses a construction method of the minipig chronic pulmonary hypertension animal model. With the adoption of the minipig chronic pulmonary hypertension animal model and the construction method thereof, the body size and structure of the minipig adopted by the minipig chronic pulmonary hypertension animal model are similar to the body size and structure of a human body, so that the minipig chronic pulmonary hypertension animal model can be determined and observed in clinic by clinical equipment; and pathological changes of the minipig chronic pulmonary hypertension animal model approach to clinical pathological changes of human beings, thus being beneficial for observation, treatment and research for a long time.
US6911476 Useful for potentiating glutamate receptor function therefore useful for treating a wide variety of conditions, such as psychiatric and neurological disorders The present invention provides certain sulfonamide derivatives useful for potentiating glutamate receptor function in a patient and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
CN101455661B Use of 3-substituted phthalide and the analogue The present invention relates to the use of 3-sbustituted phthalide or analogue for preparing the medicine for treating Alzheimer disease or other neurotic disease. The structural formula is shown in the following formula: formula (1), formula (2) or formula (3). Filtering is executed through a high-effective living model which integrates gene technique and biological technique. The research shows that most compounds have a certain function that the defective individual recovers learning capacity, wherein a plurality of specific compounds represent better activity. The learning capacity of deflective individual can be recovered for above 85%. Furthermore a stable treating effect can be shown in a plurality of tests.
US20050267156 Broadspectrum 2-amino-benzothiazole sulfonamide hiv protease inhibitors The present invention relates to the use of 2-amino-benzothiazoles, having the formula wherein R1 is hexahydrofuro[2,3-b]furanyl, tetrahydrofuranyl, oxazolyl, thiazolyl, pyridinyl, or phenyl optionally substituted with one or more substituents independently selected from C1-6alkyl, hydroxy, amino, halogen, aminoC1-4alkyl and mono- or di(C1-4alkyl)amino; R2 is hydrogen or C1-6alkyl; L is a direct bond, —O—, C1-6alkanediyl-O— or —O—C1-6alkanediyl; R3 is phenylC1-4alkyl; R4 is C1-6alkyl; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; in the manufacture of a medicament useful for inhibiting mutant HIV protease in a mammal infected with said mutant HIV protease. It also relates to novel compounds of formula (I).
CN101474156B Vitamin C precursor liposome and preparation method thereof The invention relates to the technical fields of medicament and cosmetics, in particular to a vitamin C proliposome and a preparation method thereof. The vitamin C proliposome can be used for preparing a transdermal preparation and cosmetics. The vitamin C proliposome is a solid granular preparation which ensures that the stabilities of the vitamin C and the proliposome are improved, and the vitamin C proliposome can revert to a vitamin C lipidosome only by adding a small amount of water or aqueous solution for hydration before the vitamin C proliposome is in use, and thereby, a sufficient amount of vitamin C lipidosome is added into the transdermal preparation and the cosmetics according to need so that the content of the vitamin C in the transdermal preparation and the cosmetics reachesthe required dosage, and thereby, the efficacy is improved.
WO2006022374A1 2-phenylpyridine derivative A 2-phenylpyridine derivative represented by the following general formula (I) or a salt thereof. The compounds have satisfactory xanthine oxidase inhibitory activity and uric acid-lowering activity and are useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory intestinal diseases, diabetic nephropathy, diabetic retinopathy, etc. [The symbols in the formula have the following meanings: R1: H, etc.; R2: -CO2H, etc.; R3 and R4: H, etc.; R5: -CN, etc.; R6: H, etc.; X: -O-, -N(R8)-, or -S-; (provided that the groups represented by R5 and -X-R7 are bonded in a meta position or the para position to the pyridyl group) R8: H, etc.; R7: C1-8 linear or branched alkyl, etc.; Y: a bond, etc.; and R9, R10, and R11: H, etc. (provided that when X is -N(R8)-, then R8 may be bonded to R7 to form a nitrogenous saturated heterocycle in cooperation with the adjacent nitrogen atom).]
WO2010073034A1 Pyrimidine indole derivatives for treating cancer There is provided pyrimidinyl indole compounds of Formula (I), or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly for treating cancer.
CN103585152A Application of Caesanines D in medicament for treating rhinitis The invention discloses a Caesanines D for treating immune-inflammation, for preparing a medicament for curing immune-inflammation, and particularly for preparing a medicament for curing rhinitis. Terfenadine and diclofenac sodium are taken as control, Caesanines D is explicit in curative effect and is issued for the first time, because of the novel framework type and the high rhinitis treatment activity, Caesanines D has outstanding substantive characteristics, and meanwhile the prevention and the treatment on rhinitis are greatly improved.
EP1874783B1 Substituted oxa-diaza-spiro-[5.5]-undecanone derivatives and their use as neurokinin antagonists This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK1 antagonistic activity, an NK3 antagonistic activity, a combined NK1/NK2 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incont inence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
US20090082264 123 Human Secreted Proteins The present invention relates to novel human secreted proteins and isolated nucleic acids containing the coding regions of the genes encoding such proteins. Also provided are vectors, host cells, antibodies, and recombinant methods for producing human secreted proteins. The invention further relates to diagnostic and therapeutic methods useful for diagnosing and treating diseases, disorders, and/or conditions related to these novel human secreted proteins.
US7910551 Gene differentially expressed in breast and bladder cancer and encoded polypeptides The present invention relates to a novel human gene that is differentially expressed in human carcinoma. More specifically, the present invention relates to methods of treating or preventing a disorder in a subject. The invention further relates to uses of C35 polypeptides in immunogenic compositions or vaccines, to induce antibody or T cell-mediated immunity against target cells, such as tumor cells, that express the C35 gene. The present invention further relates to use of C35 polypeptides in diagnosing a pathological condition or susceptibility to a pathological condition in a subject.
CN102274158B Prulifloxacin liposome gel and preparation method thereof The invention discloses a prulifloxacin liposome gel and a preparation method thereof. The gel is prepared from the following raw materials: 1-2 parts by weight of prulifloxacin, 10-40 parts by weight of lecithin, 2-8 parts by weight of cholesterol, and a mixed buffer solution of Na2HPO4 and NaOH with the pH of 10-11. The prulifloxacin liposome gel, which has a particle size range of 2-6nm and anaverage entrapment rate of near 70%, and possesses obvious slow release effects and stable activities, can be treated as a new dosage form of prulifloxacin on clinic.
CN103381145A Method for improving levodropropizine taste by solid dispersion The invention discloses a method for improving a levodropropizine taste by solid dispersion. The method comprises the step that levodropropizine is dispersed in one or more difficultly-dissolved auxiliary materials so that a solid dispersoid is produced, wherein the one or more difficultly-dissolved auxiliary materials are selected from difficultly-dissolved materials such as polyethylene glycol, povidone, organic acids, surfactants, cellulose, cellulose derivatives, ethyl cellulose, polyacrylic resin and sugar alcohol. The solid dispersoid is a difficultly-dissolved material and thus when a drug prepared from the solid dispersoid passes through a patient mouth cavity, dissolved levodropropizine is less so that the patient does not feel a peculiar smell and a bitter taste. Therefore, a levodropropizine taste is improved effectively and patient compliance is improved. The solid dispersoid of levodropropizine does not influence levodropropizine curative effects and can effectively improve levodropropizine clinical application.
WO2009052625A1 Novel crystalline salts of montelukast The present application relates to crystalline 1,2-ethanedisulfonic acid salt and N,N'-dibenzylethylenediamine salt of montelukast. The salts are useful as therapeutic agents for the treatment of leukotriene mediated diseases and disorders. This application also relates to processes and intermediates for preparing the said salts and pharmaceutical compositions comprising the salts and optionally other therapeutic agents.
WO2006088694A1 SUBSTITUTED THIENYL AND FURYL ACYLGUANIDINES AS β-SECRETASE MODULATORS The present invention provides a substituted thienyl or furyl acylguanidine compound of formula I. The present invention also provides methods for the inhibition of β-secretase (BACE) and for the treatment of β-amyloid deposits and neurofibrillary tangles.
WO2008075109A1 Substituted piperidines having protein kinase inhibiting activity The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I); or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group CR5; J1-J2 is N=C(R6), (R7)C=N, (R8)N- C(O), (R8)2C-C(O), N=N or (R7)C=C(R6); Q3 is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR2R3, CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R1a and R1b are the same or different and each is hydrogen or a substituent R10; or R1a and R1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R10; and R2, R3, R4, R5, R7, R6, R8, and R10 are as defined in the claims.
US20080167320 Compounds are selective ligands for the dopamine D3 receptor; psychotic or depressive disorders, dyskinesia, essential tremor; 2-{4-[4-(3-trifluoromethylphenyl)piperazin-1-yl]butyl}amino-4-phenylpyridine; neuropsychiatry; drug dependency/abuse Compounds of the general formula (I) below: are provided along with a process for preparing them, and these compounds may be used as therapeutic agents, e.g., for prevention and/or treatment of a neuropsychiatric illness or any illness involving the dopamine D3 receptor.
DE102004061503A1 New meta-substituted thiazolidinone compounds are polo-like kinase inhibitors useful to treat cancers, autoimmune-, cardiovascular-, infectious-, nephrological-, nephrological- and neurodegenerative-diseases Meta-substituted thiazolidinone compounds (I), their solvates, hydrates, diastereomers, enantiomers and salts are new. Meta-substituted thiazolidinone compounds of formula (I), their solvates, hydrates, diastereomers, enantiomers and salts are new. T1>, T3>-CH= or -N=; T2>T1> or (-CF)=; U1>e.g. -N=; R1>1-3C alkyl or cyclopropyl (both optionally substituted with halo); R2>1-3C alkyl, 3-4C alkenyl, 3-4C alkynyl or cyclopropyl (all optionally substituted with CN, cyclopropyl, ethynyl or halo); R3>e.g. K1>; and K1>1-3C alkyl or 2-4C alkenyl (both optionally substituted). Full definitions are given in the DEFINITIONS - Full Definitions section. Independent claims are also included for: (1) substituted thiazolidinone compounds of formula (II) or (IV), their solvates, hydrates, diastereomers, enantiomers and salts as intermediates for preparing (I); and (2) the preparation of (I). [Image] [Image] - ACTIVITY : Cytostatic; Immunosuppressive; Antipsoriatic; Endocrine-Gen.; Neuroprotective; Cardiovascular-Gen.; Antiarteriosclerotic; Vasotropic; Antimicrobial; Antiparasitic; Nephrotropic; Anticonvulsant; Nootropic; Antiparkinsonian; Virucide; Antiinflammatory; Hepatotropic; Anti-HIV. - MECHANISM OF ACTION : Polo-like kinase inhibitor.
CN101361734A Alpha-linolenic acid complexing agent An Alpha- linolenic acid complexing agent contains 60-80g of Alpha-linolenic acid that is an active ingredient, 10-15mg of vitamin A, 200-500mg of vitamin C and 1-4g of vitamin E per kg. In the invention, the Alpha- linolenic acid complexing agent is made into a dripping pill by regular preparation process. Proved by the research on the effects of the Alpha- linolenic acid complexing agent on the blood-fat content in the serum of an elderly mouse, resisting free radicals and prolonging the life of fruit flies and on the expression change of telomere enzyme mRNA in the liver of a mouse, the Alpha- linolenic acid complexing agent has the efficacies of reducing blood-fat, resisting free radicals, deferring senility and prolonging the life.
US20110159094 Extended release compositions for high solubility, high permeability active pharmaceutical ingredients A novel composition comprising a tablet, comprising a highly soluble active pharmaceutical ingredient, which is then coated with a coating. The core is preferably a tablet. The coating preferably comprises any type of suitable extended release polymer, with the proviso that the polymer does not comprise an enteric polymer.
US20120308542 Method for Ameliorating or Preventing Arrhythmic Risk Associated with Cardiomyopathy by Improving Conduction Velocity A method for reducing arrhythmic risk associated with cardiomyopathy by improving conduction velocity, includes administering a composition containing NAD+ or a mitochondrial targeted antioxidant to an individual or person in need thereof.
CN103110642A Cefonicid sodium drug composition and preparation method thereof The invention provides a cefonicid sodium drug composition and a preparation method thereof, relating to the fields of pharmaceutical preparations and preparation methods and mainly solving the problems that single preparations of cefonicid sodium and metronidazole in the prior art have great dosages, poor treatment effects after being combined and big side effects. The drug composition comprises cefonicid sodium and metronidazole lipid microspheres in a weight ratio of (100:3)-(100:10), wherein the weight of the metronidazole lipid microspheres is based on metronidazole. The drug composition is prepared into powder injection. The pH value of water solution of the drug composition is 6.5-7.0. The powder injection of the drug composition provided by the invention not only has high curative effect but also can reduce the dosage of metronidazole by over 80%, thus greatly reducing or avoiding the toxic and side effects, especially gastrointestinal reactions including nausea, emesis, anorexia, abdominal cramp and neurotoxicity, of metronidazole and further reducing the occurrence rate of adverse reactions.
CN101406476A Agent for treating skin peeling and allergy The invention relates to a medicament for treating peeling and sensibility of skin, which is prepared from raw materials in the following weight ratio after being ground into powders and mixed: 1 to 10 portions of dexamethasone acetate, 1 to 3 portions of diphenhydramine hydrochloride, 5 to 15 portions of triamcinolone acetonide acetate, 900 to 1,200 portions of carbamide, 20 to 40 portions of vitamin A, and 21 to 5 portions of vitamin D. Compared with the prior medicament for treating skin peeling and dead skin, the medicament has the advantages of rapid effect, definite curative effect, non-allergenic and non-irritating properties, no toxic side effects and the like, and the medicament can achieve the aim of beauty and skin care.
CN1634073A Orally disintegrating tablet of levofloxacin and its pharmaceutical salt The invention relates to an orally disintegrating tablet of levofloxacin and its pharmaceutical salt which comprises physiologically effective amount of Levofloxacin or its medicinal salts and / or pharmaceutically acceptable carriers suitable for preparing orally disintegrating tablet, wherein the pharmaceutically acceptable carriers suitable for preparing orally disintegrating tablet include macromolecular material, bulking agent, crumbling agent, effervescent agent, lubricating agent, flavoring agent and other pharmaceutically acceptable carriers suitable for preparing orally disintegrating tablets.
CN101401803A Uses of 2,5-dewatering-D-glucitol and the like in preparing cancer treatment medicament The invention discloses novel application of 2, 5-dehydrated-D-glucitol and an analogue thereof in the preparation of medicaments for treating cancer. The 2, 5-dehydrated-D-glucitol, 2, 5-dehydrated-1-deoxy-D-glucitol and 2, 5-dehydrated-D-gluconic acid can significantly inhibit and kill tumor cells.
CN102284001B Compound rhizoma polygonati oral liquid and preparation method thereof The invention discloses compound rhizoma polygonati oral liquid and a preparation method thereof. The compound rhizoma polygonati oral liquid is prepared from rhizoma polygonati, Astragalus mongholicus, Semen Cuscutae, herba epimedii, Radix Ophiopogonis, Morinda officinalis, stilbene and sodium benzoate. The compound rhizoma polygonati oral liquid disclosed by the invention has an effect of effectively enhancing the organism immunity. Shown by the researches of experimental pharmacology and clinical therapeutics, the compound rhizoma polygonati oral liquid has an anti-tumor action on a Lewis mouse with lung cancer and is capable of increasing the thymus index, the spleen index and the CD4<+>/CD8<+> specific value of the mouse, thus, the compound rhizoma polygonati oral liquid has the effect of enhancing the organism immunity. The compound rhizoma polygonati oral liquid is also capable of improving the interleukin-2 (IL-2) level of the serum of the mouse, promoting the recovery of the white blood cells of the mouse, enhancing the (superoxide dismutase) SOD activity of the serum and reducing the malondialdehyde (MDA) content of the serum and has anti-inflammatory and antioxidation actions.
CN103446117A Applications of Sarcaboside A in medicament against helicobacter pylori The invention relates to applications of Sarcaboside A in a medicament against helicobacter pylori. In-vitro activity experiments show that the Sarcaboside A has strong activity against the Helicobacter pylori Hp. The Sarcaboside A can be used for treating diseases of acute and chronic gastritis, gastric ulcer, duodenal ulcer and the like, and can be applied to preparing medicaments for preventing acute and chronic gastritis, gastric ulcer and duodenal ulcer. The applications of the Sarcaboside A in the medicament against helicobacter pylori are disclosed for the first time. As a skeleton type of the Sarcaboside A belongs to a brand-new skeleton type, the Sarcaboside A has unexpectedly strong helicobacter pylori inhibition activity, and the possibility of giving any inspiration by other compounds does not exist. The Sarcaboside A has significantly substantive characteristics, as well as obviously prominent progress in the prevention and treatment of the helicobacter pylori infection.
EP1497288A1 Novel ester hydroxy-substituted nitrogen heterocycles as antagonists of the muscarinic m3 receptor, methods for the production thereof, and use thereof as a medicament The invention relates to novel compounds of general formula 1, in which X- and the radicals A, B, R, R1, R2, R3, R3', R4, R4', Rx, and Rx' can have the meanings mentioned in the claims and in the description, methods for the production thereof, and the use thereof as a medicament.
US20080261882 Methods for Inhibiting Heregulin and Treating Cancer The present invention discloses a method using human soluble ErbB3, for example p85-sErbB3, as a negative regulator of heregulin-stimulated ErbB2, ErbB3, and ErbB4 activation. The present invention also discloses p85-sErbB3 binding to heregulin with an affinity comparable to that of full-length ErbB3, and competitively inhibiting high affinity heregulin binding to ErbB2/ErbB3 heterodimers on the cell surface of breast carcinoma cells. The present invention also uses p85-sErbB3 to inhibit heregulin-induced phosphorylation of ErbB2, ErbB3, and ErbB4 in cells, as a negative regulator of heregulin-stimulated signal transduction, and as a block for cell growth. The present invention is also directed to nucleic acids and expression vectors encoding p85-sErbB3, host cells harboring such expression vectors, and methods of producing the protein. The present invention discloses a method of therapeutically treating human malignancies associated with heregulin-mediated cell growth such as breast and prostate cancer.
CN101129391A Medicament for eliminating OH free radical The invention discloses a drug to remove OH free radical, which comprises one of the following parts: salidroside, 6-deoxycatalpol, gluroside, bartsioside, Tubuloside A and cistantubuloside A. The invention removes OH free radical in the human body to delay senescence, which modifies the action of study and memory.
EP2568989A1 Lanthanum carbonate hydroxide, lanthanum oxycarbonate and methods of their manufacture and use The present invention is a method of producing a lanthanum carbonate hydroxide or lanthanum oxycarbonate which has improved properties. The method involves the use of a water soluble lanthanum and a water soluble non-alkali metal carbonate or bicarbonate. The resulting material can be used as a phosphate binder individually or for treating patients with hyperphosphatemia.
CN102351854A Amino thiazole derivative and preparation method and medical purpose thereof The invention provides an amino thiazole derivative compound, a tautomer thereof, a medicinal salt thereof and a preparation method thereof. The amino thiazole derivative compound, the tautomer thereof, or the medicinal salt thereof provided by the invention has effects of inhibiting acetylcholinesterase and senile plaque aggregated by beta- amyloid (A beta), and can be used for treating, improving or preventing cognitive decline related neurological diseases, such as Alzheimer disease, vascular dementia, slight cognitive impairment and other dementia with oxidative stress participation.
CN101367804B Penem derivant containing adamantane The present invention belongs to the technical field of medicine, and in particular relates to a penem derivative containing Adamantanes as shown in Formula (I), acceptable salt thereof in pharmacy, easily hydrolyzed ester thereof, isomer thereof, hydrate thereof, and hydrate of ester or salt thereof; wherein, R<1>, R<2>, R<3> and R<4> are defined as in the specification. The present invention also relates to the preparation methods of the compounds, drug compositions of the compounds, and application of the compounds in preparation of medicine which is used for treating and/or preventing infectious diseases.
WO2010146125A1 Ester derivatives as competitive inhibitors of type ii dehydroquinase enzyme The present invention is directed to a compound of formula I, its diastereoisomers, its enantiomers or its pharmaceutically acceptable salts or solvates, to procedures of obtaining the same, and use as competitive inhibitors of the third enzyme of the shikimic acid pathway, the type II dehydroquinase.
CN103720695A Drug combination containing cefdinir The invention discloses a drug combination containing cefdinir. The drug combination has the beneficial effect of great stability.
CN101653611B Albumin-adriamycin nano preparation, preparing method and application thereof The invention belongs to the technical field of medicine, in particular to an albumin-adriamycin nano preparation with double polysaccharide casing, a preparing method and application thereof. The nano preparation is the nano particle solution taking chitosan and glucan as the casing and taking albumin and adriamycin as the core. The preparing steps are as follows: mixing and heating chitosan andalbumin-glucan covalent compound to form the nano particle solution taking albumin as the core and taking glucan and chitosan as the casing; under the acidity condition, mixing the above nano particle solution and doxorubicin hydrochloride solution; under certain pH value, covering adriamycin in the nano particle by diffusion. The tumor targeting ability of the albumin of the invention can improve the curative effect of adriamycin and lower the toxic and side effect of adriamycin. The chitosan on the surface of the nano particle also has the function of resisting tumor and can strengthen immunity; glucan can prevent the nano particle from quickly clearing by macrophage so as to increase the chance for the nano particle to reach the tumor.
CN103446109A Applications of Sarcaboside B in medicament against mycobacterium tuberculosis The invention discloses applications of Sarcaboside B in preparing a medicament against mycobacterium tuberculosis. Aiming at the current situation that the occurrence of high tuberculosis incidence and multi-medicament-resistant strains of mycobacterium tuberculosis causes the rise trend of tuberculosis incidence and death rate, people discover that the Sarcaboside B has the remarkable mycobacterium tuberculosis inhibition activity and excellent application prospects. The applications of the Sarcaboside B in preparing the medicament against mycobacterium tuberculosis are disclosed for the first time. As a skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpectedly strong mycobacterium tuberculosis inhibition activity, and the possibility of giving any inspiration by other compounds does not exist. The Sarcaboside B has significantly substantive characteristics, as well as obviously prominent progress in the prevention and treatment of the mycobacterium tuberculosis infection.
EP2042164A1 Stabilized solid preparation A stabilized solid preparation having stabilized drug content and stabilized appearance, comprising a main ingredient layer and a coating layer formed on the main ingredient layer, wherein the main ingredient layer comprises a granule or a fine particle comprising a substance capable of being unstabilized when losing water of crystallization and a water-soluble polymer and the coating layer comprises a water-soluble polymer and a sugar.
US20050137237 Triazolo-epothilones The invention relates to triazolo-thiazole analogues of epothilone A and epothilone B.
EP2767541A1 LPA receptor agonists and antagonists Disclosed are compounds according to formula (I) as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including treating cancer, producing radioprotection and/or radiomitigation, enhancing cell proliferation, treating a wound, treating apoptosis or preserving or restoring function in a cell, tissue, or organ, culturing cells, preserving organ or tissue function, and treating a dermatological condition.
US8853271 Method for inhibiting activity and/or expression of matrix metalloproteinase, inhibiting phosphorylation of mitogen-activated protein kinase, and/or promoting expression of collagen using tormentic acid A method for inhibiting the activity of matrix metalloproteinase (MMP), inhibiting the expression of matrix metalloproteinase, inhibiting the phosphorylation of mitogen-activated protein kinase (MAPK), and/or promoting the expression of collagen in a mammal is provided. The method comprises administrating to the mammal an effective amount of an active component selected from a group consisting of a compound of formula (I), a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable ester of the compound, and combinations thereof:
WO2012146383A1 Tapentadol for preventing and treating depression and anxiety The invention relates to tapentadol (i) for use in the treatment of pain in a subject suffering from depression and/or from anxiety, and/or (ii) for use in the treatment or the prevention of depression and/or of anxiety.
CN101637452B Atorvastatin calcium dried suspension and preparation method thereof The invention relates to an atorvastatin calcium dried suspension and a preparation method thereof. The atorvastatin calcium dried suspension comprises the following components in portion by weight: 1 to 10 portions of atorvastatin calcium, 10 to 95 portions of filling agent, 1 to 30 portions of suspension and/or suspending agent, 2 to 40 portions of flavoring agent, and 0.2 to 2.0 portions of lubricating agent. The atorvastatin calcium dried suspension has the advantages of high dispersity, even distribution, quick absorption, high bioavailability, good adaptability, good mouthfeel, stability and the like. The atorvastatin calcium dried suspension can be applied to regulation of blood fat.
US20070259890 Compounds and Compositions as Ppar Modulators The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPARδ.
WO2010018481A1 2-amino pyrimidine compounds as potent hsp-90 inhibitors The present invention is directed to compounds of Formula (I), or pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors in the treatment of proliferative diseases, e.g. cancer.
CN101204367A Axitinib sustained-release implplant treating for solid tumor The invention relates to an Axitinib sustained-release implant for treating a solid tumor, which is characterized in that: the sustained-release implant contains an effective anticancer amount of Axitinib and sustained-release excipients and a certain amount of sustained-release regulator. The solid tumors include the liver cancer, the lung cancer, the esophageal canner, the gastric canner, the breast canner, the ovarian canner, the prostate canner, the bladder canner and the rectum canner. The sustained-release excipients are mainly a copolymer of polylactic acid, glycollic acid and hydroxyacetic acid and one of the three materials, polifeprosan, poly-(L-lactide-co-ethyl phosphonate) and Poly(L-lactide-co-propyl phosphonate) or a combination of the three materials, in the degradation and absorption process of which the Axitinib is sustainedly released to part of the tumor, thus the entire toxicity of the Axitinib is significantly reduced while an effective medicine consistency is maintained on part of the tumor. That the sustained-release implant is implanted inside part of the tumor can not only reduce the entire toxicity of the Axitinib, but also enhance the medicine consistency on part of the tumor, thereby increasing the curing effect of non-operative therapeutics such as chemotherapeutic drugs and radiotherapy.
WO2009018405A1 Integrated photoactive agents and uses thereof The present invention discloses a number of photoactive compounds designed to bind and inhibit serine proteases. Compounds disclosed herein may be utilized in a number of appropriate medical diagnostic and/or therapeutic procedures such as the monitoring of hemostasis, imaging and/or treatment of vulnerable plaques, and/or tumor imaging and/or treatment.
EP2338490A2 Combinations Useful for the Treatment of Neuronal Disorders The present invention provides a method for the treatment of neuronal disorders, in a mammal such as a human, which method comprises administering an effective, nontoxic and pharmaceutically acceptable amount of at least one QC-inhibitor, optionally in combination with at least one agent, selected from the group consisting of PEP-inhibitors, inhibitors of DP IV/DP IV-like enzymes, NPY-receptor ligands, NPY agonists, NPY antagonists, ACE-inhibitors, PIMT enhancers, inhibitors of beta secretases, inhibitors of gamma secretases and inhibitors of neutral endopeptidase, to a mammal in need thereof.
WO2008076000A1 Agent for treating acute intoxications and complication thereof The invention relates to the use of acizol in the form of an agent for preventing and treating intoxications produced by combustion products, thermal destruction and by neurotoxic substances. The high efficiency of acizol for comprehensively treating toxico-hypoxic encephalopathy and pneumonia (homeostasis normalisation, reduction of mortality and incapacitating complications) is also disclosed.
CN102772383A Azithromycin composition freeze-dried orally disintegrating tablet and preparation method thereof The invention discloses an azithromycin composition freeze-dried orally disintegrating tablet and a preparation method thereof, relates to the technical field of medicines and preparation methods thereof, and mainly solves the problems that the production process and the azithromycin preparation components are complicated, and the disintegrating tablet is low in disintegrating speed in the prior art. The azithromycin composition freeze-dried orally disintegrating tablet comprises the following components in percentage by weight: 10 to 24 percent of azithromycin, 24 to 50 percent of mannitol, 2 to 4 percent of gelatin, 32 to 74 percent of middle-substitution-degree hydroxypropyl-beta-cyclodextrin, 0.1 to 0.2 percent of sucralose and 50 percent of purified water. The preparation process of the azithromycin composition freeze-dried orally disintegrating tablet prepared by the components is simple, and the components are simple; and the azithromycin preparation can reduce the side effect of azithromycin, is convenient to take and tastes good.
CN101559098A Chinese patent medicine for treating scapulohumeral periarthritis The invention belongs to a Chinese patent medicine for treating scapulohumeral periarthritis, which is prepared from medicines comprising notopterygium root, heracleum hemsleyanum michaux, borneol, lycopodium calvatum, asarum, rhizoma ligustici wallichii, cinnamon, frankincense, myrrh, sapanwood, and the like. The Chinese patent medicine has no toxic or side effect, expels wind, clears away cold, promotes blood circulation by removing blood stasis, has obvious effect and cures arthropathy rapidly.
US20060194874 Use of propionyl l-carnitine for the preparation of a medicament for the treatment of glaucoma Propionyl L-carnitine is used for the treatment of glaucoma and is preferably administrated orally or ophthalmically. Propionyl L-carnitine exhibits an anti-aptoptotic action on the nerve cells of the eye.
CN103356488A Capecitabine granule and preparation method thereof The invention relates to an oral anti-tumor drug capecitabine granule and a preparation method thereof. The capecitabine granule exists in the form of a cyclodextrin inclusion compound and is prepared from capecitabine serving as a raw material drug and auxiliary materials comprising cyclodextrin, a diluting agent, a disintegrating agent, an adhesive and a flavoring agent by wet granulation. The capecitabine granule disclosed by the invention not only covers the bitterness of a capecitabine drug and enhances the drug compliance of a cancerous person, but also enhances the stability of the capecitabine in gastrointestinal tracts and accelerates the digestion velocity, thereby preventing the peak valley phenomenon of the blood concentration of a drug, outstandingly reducing the adverse reactions of the drug, such as irritation and toxic side effect, on the gastrointestinal tracts due to the stable release of capecitabine in the gastrointestinal tracts, enhancing the drug safety and better taking the anti-tumor effect.
US20080032939 Iridoid-saccharide compound and method of using same A method for treatment of hyperproliferative tissue which by exposing the hyperproliferative tissue to a sufficient quantity of a purified iridoid compound to inhibit its growth, where the iridoid compound includes a polysubstituted cyclopenta(c)dihydropyran where the cyclopenta ring is substituted at its 2′ position with a ketofuryl group, where the numbering of the fused cyclopenta(c)dihydropyran ring structure includes heterocyclic oxygen, is counterclockwise and begins at the first carbon atom counterclockwise from the cyclopenta ring so that oxygen is in the 2 position in the pyran ring. The invention also includes the mouse iridoid compounds.
US20080207594 Glycogen synthase kinase inhibitor in mixture with immunomodulating agents; antidiabetic agents; immunosupprsants This invention relates to the use of Pax4 stimulating compounds, e.g. Glycogen synthase kinase-3 (GSK-3) inhibitors, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA. More particularly, this invention relates to the use of compounds selected from paullones, indirubines, substituted ureas, maleimide derivatives and pyrimidine thiones. Further, the present invention relates to a method of identifying and/or characterizing pancreatic beta-cell mitogens by using cells expressing a pancreatic gene or a gene whose function is controlled by a pancreatic gene, particularly the Pax4 gene, and which are transfected with a reporter gene.
US7439359 Antiproliferative agents; antitumor agents; binding to chaperone protein Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with an affinity which is greater than ADP and different from the ansamycin antibiotics for at least one species of the HSP90 family. Moreover, these small molecules can be designed to be soluble in aqueous media, thus providing a further advantage over the use of ansamycin antibiotics. Pharmaceutical compositions can be formulated containing a pharmaceutically acceptable carrier and a molecule that includes a binding moiety which binds to the N-terminal pocket of at least one member of the HSP90 family of proteins. Such binding moieties were found to have antiproliferative activity against tumor cells which are dependent on proteins requiring chaperones of the HSP90 family for their function. Different chemical species have different activity, however, allowing the selection of, for example Her2 degradation without degradation of Raf kinase. Thus, the binding moieties possess an inherent targeting capacity. In addition, the small molecules can be linked to targeting moieties to provide targeting of the activity to specific classes of cells. Thus, the invention further provides a method for treatment of diseases, including cancers, by administration of these compositions. Dimeric forms of the binding moieties may also be employed.
WO2007109845A1 Prophylaxis or treatment of diabetes Methods for prophylaxis or treatment of diabetic or pre-diabetic conditions are described. The methods comprise administering a therapeutic amount of a complex of metal and a carboxylate, or a derivative of a carboxylate, having anti-inflammatory activity.
WO2014009500A1 Anti-tumoral composition comprising the compound 1-(6-{[6-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl}-1,3-benzothiazol-2-yl)-3-(2-morpholin-4-ylethyl)urea The present invention concerns an anti-tumoral composition comprising the compound 1-(6-{[6-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl}-1,3- benzothiazol-2-yl)-3-(2-morpholin-4-ylethyl)urea and its use in the treatment of cancer.
CN1867559A Glutamine fructose-6-phosphate amidotransferase (GFAT) inhibitors Compounds of formula (I) are provided, wherein R<1> and R<2> are as designated in the specification. The compounds have utility for the treatment of type 2 diabetes mellitus.
CN103755801A Application of combination of earthworm fibrinolytic-activity protein and paclitaxel in preparing drugs for inhibiting cancer cells The invention discloses an earthworm fibrinolytic-activity protein which is prepared by the following steps: taking verdure earthworm, adding water, homogenating, standing, centrifugating to obtain a protein supernate, salting out, centrifugating, and dissolving the precipitate in water to obtain an earthworm fibrinolytic-activity protein crude extract; carrying out dialytic desalting, anion exchange chromatography, gel filtration chromatography, gel column desalting impurity removal and freeze-drying on the crude extract to obtain solid powder, and screening the active protein by cell experiments in the separation process to finally obtain the purified earthworm fibrinolytic-activity protein. The experimental research detects that the combination of the earthworm fibrinolytic-activity protein and paclitaxel can inhibit growth of the tumor cells in vitro, and thus, can be used for preparing drugs for inhibiting cancer cells. The invention also discloses a combined drug for inhibiting tumor cells, which comprises the earthworm fibrinolytic-activity protein and paclitaxel, and optionally one or more drug carriers.
CN1879613A Medicine containing galangin and preparation method thereof The invention relates to a medicine that contains galangal rhizome and relative preparation, wherein the galangal rhizome chromocor separated from the root of galangal rhizome contains chromocor at 50-99.8% and galangal rhizome at 30-80%. The preparation comprises: (1) extracting, abstracting, inverted abstracting, depositing chromocor, and purifying the galangal rhizome to obtain the galangal rhizome chromocor, to be used to prepare oral or ejection agent. The invention has simple process and easy operation, while the product has high purity. And the inventive medicine can be used to resist oxidization, etc.
WO2006013546A3 Process for the preparation of pure galantamine The invention relates to processes for the preparation of pure galantamine or pharmaceutically acceptable salts thereof. More particularly, it relates to the preparation of pure galantamine hydrobromide. The invention also relates to pharmaceutical compositions that include the pure galantamine or pharmaceutically acceptable salts thereof and use of said compositions for treating Alzheimer's disease, dementia, mania, fatigue syndrome, and schizophrenia.
WO2013077830A1 Synergistilly active combinations of roflumilast and carmoterol The present invention relates to use of the selective phosphodiesterase-4 (PDE-4) enzyme inhibitor roflumilast and the β2-adrenergic receptor agonist carmoterol in combined form and pharmaceutical drug compositions comprising said pharmaceutical composition which can be used in allergic and inflammatory diseases of skin and upper and lower respiratory tracts.
CN101366711B Taurine and common oats fibre compound formulation, and uses thereof The invention relates to the technical field of medicine and pharmacology, in particular to a compound peroral preparation consisting of taurine and oak fibers and application of the compound peroral preparation in inhibiting absorption of intestinal endotoxin. The invention adopts a reflow model of mouse portal vein blockage to develop the inhibition effect of the compound peroral composition consisting of the taurine and the oak fibers on the absorption of the intestinal endotoxin. As shown by the result, the compound preparation of the taurine and the oak fibers has obvious inhibition effect on the absorption of the intestinal endotoxin of the reflow model of mouse portal vein blockage; and the inhibition effect of the compound preparation is superior to that of the pure peroral taurine or the pure peroral oak fibers, which shows that the taurine and the oak fibers have synergistic reaction. Therefore the compound peroral preparation can be used for preparing medicines or foodstuffs for inhibiting the absorption of the intestinal endotoxin.
WO2005113550A1 Aminopyrimidine derivative and medicinal use thereof An aminopyrimidine compound represented by the following general formula (I), pharmaceutically acceptable salt, hydrate, water adduct, and solvate. These compounds were found to potently inhibit proteinkinases, especially aurora 2 kinase, and be capable of sufficiently acting in the living body. The invention has been thus completed. [Chemical formula 1]
WO2011061613A1 Process for the preparation of crystalline form ii of l-malic acid salt of sunitinib The present invention relates to stable crystalline Form II of L-malic acid salt of sunitinib and its preparation.
US20090227533 miR-34 Regulated Genes and Pathways as Targets for Therapeutic Intervention The present invention concerns methods and compositions for identifying genes or genetic pathways modulated by miR-34, using miR-34 to modulate a gene or gene pathway, using this profile in assessing the condition of a patient and/or treating the patient with an appropriate miRNA.
US20090221640 Novel Crystal Modifications Novel crystal modifications of (5S)-5-[4-(5-chloro-pyridin-2-yloxy)-piperidine-1-sulfonylmethyl]-5-methyl-imidazolidine-2,4-dione are disclosed together with processes for preparing such modifications, pharmaceutical compositions comprising such a modification, and the use of such a modification in therapy.
EP1812000A1 Aqueous ophthalmic suspension of crystalline rebamipide The invention provides an ophthalmic product containing rebamipide, which has a transparency enough to be agreeable feeling on using it and has neutral to weakly acidic pH not to injury of the keratoconjunctiva of a patient suffering from dry eye. An aqueous suspension of crystalline rebamipide which has an improved transparency is provided by adding an aqueous solution of rebamipide dissolved by a base such as sodium hydroxide or an aqueous solution of a salt of rebamipide to an aqueous acidic solution such as hydrochloric acid containing at least one of the compounds selected from water-soluble polymers and surfactants, and mixing them.
WO2014021383A1 Condensed ring heterocyclic compound This condensed ring heterocyclic compound or pharmaceutically acceptable salt thereof has a T-type calcium channel regulatory effect and is useful as a drug for the treatment and/or prevention of pruritus, for example. The invention provides a condensed ring heterocyclic compound represented by general formula (I) [in the formula, R1 represents an optionally substituted lower alkyl or the like, R2 represents an optionally substituted lower alkyl or the like, R3 represents formula (II) (in the formula, n represents 0 or 1, R3a represents a hydrogen atom or the like, R3b represents a hydrogen atom or the like, and R3c represents a hydrogen atom or the like) or the like, Q represents a hydrogen atom or the like, W1 represents a nitrogen atom or the like, and W2 represents a nitrogen atom or the like] or a pharmaceutically acceptable salt thereof or the like that has a T-type calcium channel regulatory effect and is useful as, for example, an agent for the treatment and/or prevention of pruritus.
CA2330007C Improvements in macrolide production A process for the production of azithromycins by methylation of the nitrogen atom in position 9 of the ring structure in 9-deoxo-9a-aza-9a-homoerythromycins in the presence of formaldehyde and in the presence of a reducing agent in non-halogenated solvent; and azithromycin which is free from halogenated organic solvent in a stable anhydrous form; or in the form of a solvate with non-halogenated solvent with the exception of water.
US20120149678 Organonitro Compounds for Use in Treating Non-Hodgkin's Lymphoma and Leukemia, and Methods Relating Thereto The invention provides organonitro compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat non-Hodgkin's lymphoma and certain leukemias in a patient. The compounds, compositions, kits, and methods are contemplated to provide a therapeutic benefit in treating non-Hodgkin's lymphoma, chronic lymphocytic leukemia, acute myelogenous leukemia, chronic myelogenous leukemia, and acute lymphoblastic leukemia. Exemplary organonitro compounds described herein include alkyl-substituted and acyl-substituted di-nitroheterocycles.
CN1810249A Soft medicine composition capsule and its prepn The present invention relates to soft medicine composition capsule with Itraconazole as the active matter and its preparation process. The soft medicine composition capsule has content mixture comprising Itraconazole, diluent, co-solvent, solubilizer and surfactant. It has high medicine stability, high medicine safety and high medicine effectiveness.
CN101199507A Application of furan diene and derivatives in preparing therapeautic cancer medicament The invention relates to an application of furanodiene and derivatives of the furanodiene in preparing drugs for treating cancer, in particular to an application in preparing drugs for treating cervical cancer, laryngeal carcinoma, leukemia, glioma, ascites carcinoma, lung cancer, gastric cancer, prostate cancer and liver cancer. The invention also relates to drugs which adopt furanodiene as an active component to treat cancers.
CN102114026A Ointment preparation for treating duck leg diseases and preparation method thereof The invention relates to an ointment containing nano-scale gentamycin sulfate and cefaclor for treating duck leg diseases and a preparation method thereof. The main medicaments of the ointment preparation are nano-scale powder, the ointment preparation can be applied to skin directly, and has the advantages of strengthening the target effect of medicaments, convenient administration, quick absorption, direct achievement to deeper skin, strong sterilization, small side effect and the like. The ointment preparation can effectively treat the duck leg diseases due to duck leg infection caused by staphylococcus, pseudomonas aeruginosa and other bacteria, so that the ointment containing the nano-scale gentamycin sulfate and the cefaclor can sufficiently play the effect of the medicament when treating the duck leg diseases.
US20110177996 Regulatory proteins in lung repair and treatment of lung disease The DNA-binding protein Sox17 has been found to play an important role in repair of pulmonary tissue after damage, disease, or injury. Nucleic acids encoding proteins involved in pulmonary repair, such as Sox17 and Spdef, can be used as a therapeutic composition for treating pulmonary disease. Methods of treatment of pulmonary injuries or pulmonary diseases are also disclosed, as are methods of identifying compounds effective in treating pulmonary injuries and diseases.
US20110306668 Construction and screening of solution-phase derived library of fenbufen and ethacrynic acid A process for synthesizing and screening solution phase derived libraries of fenbufen and ethacrynic acid is provided in the present invention. Compounds in the present invention having cytotoxicities are useful for a variety of therapeutic applications.
CN101002777A Injection solution containing anti-infective medicine An injection of the quinolone medicine for treating infectionis prepared from the medicine A and the buffers solution of weak acid or its salt. Said medicine A is 6-fluoro-1-methyl, 4-oxy-7-(1-piperazinyl)-4H-[1, 3] thiazine [3, 2-a] quinoline-3- carboxylate.
EP1434590B1 Method for inhibiting the formation of seromas using factor xiii Use of factor XIII for inhibiting the formation of seromas by administering factor XIII. The factor XIII can be administered locally at the site of a wound or surgery or administered systemically. If the factor XIII is administered locally, it can be activated or nonactivated and may be administered in conjunction with activated thrombin.
CN1559429A Freezing-drying powder injectiong contg. Xi-Duo-Fu-Wei A Xiduofuwei injection in the form of freeze-dried powder for treating AIDS, cytomegalovirus infection of retina, hepes, simplex virus infection, variola virus infection, etc is prepared from Xiduofuwei, and excipient through proportional dissolving, regulating pH value, filter, quickly freezing, heatingand sublimation drying.
WO2007068948A3 Pharmaceutical sustained release compositions comprising in particular thyroid hormones There is provided sustained release pharmaceutical compositions comprising a drug; microcrystalline cellulose; a diluent (such as starch); a glidant (such as talc); and one or more of ethylcellulose, stearic acid and a salt of stearic acid. Preferred drugs include those that exhibit a low degree of solubility combined with a high potency, particularly thyroid hormones, such as liothyronine.
US20090098105 Treatment of neurodegenerative diseases by the use of scd4 inhibitors The present invention relates to the use of SCD4 interacting molecules, especially SCD4 inhibitors, for the preparation of a medicament for the treatment of neurodegenerative diseases, particularly Alzheimer's disease.
US7803835 Substituted acetic acid derivatives The present invention relates generally to substituted acetic acid derivatives and methods of using them.
US7229646 Methods and compositions for modulating immune response and for the treatment of inflammatory disease Compositions and methods for treating inflammatory disease and for modulating the immune system are described. The compositions and methods pertain to the use of a combination of N,N-dimethylglycine and a component derived from the mussel Perna canaliculus to achieve synergistic anti-inflammatory and immunomodulating effects.
WO2010027448A8 Isotopically enriched pyrimidin-5-yl acetic acid derivatives as crth2 antagonists Provided herein are 2H- and 13C-enriched compounds of formula (I) or (II); wherein R is as defined herein, and wherein at least one hydrogen atom, in certain embodiments, three or more hydrogen atoms, are deuterium atoms or at least one carbon atom is a carbon- 13 atom. Also provided are pharmaceutical compositions and methods using the 2H- and 13C-enriched compounds, useful for treating CRTH2-related diseases or disorders such as, for example, asthma, allergic rhinitis, atopic dermatitis, allergic conjuvatitis, Churg-Strauss syndrome, sinusitis, basophilic leukemia, chronic urticaria or basophilic leukocytosis.
WO2012143399A1 Substituted 4-aryl-n-phenyl-1,3,5-triazin-2-amines The present invention relates to substituted 4-Aryl-N-phenyl-1,3,5-triazin-2-amines of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
US6989155 Particles comprising amino acid such as leucine and optionally with drug mixtures formed by aerosol condensation or spray drying, for use as inhalants; antiasthmatics Particles of an amino acid such as leucine may be formed from an amino acid vapor, for example by aerosol condensation, or by spray drying. The amino acid particles have a bulk density of not more than 0.1 gcm−3 or have a mass median aerodynamic diameter of not more than 10 μm or are in the form of flakes having a thickness of not more than 100 μm. The inclusion of the particles of amino acid in powder for use in dry powder inhalers has been found to improve the respirable fraction of the active material in the powder.
CN1548413B Beta-diketoacid as dimer compound and its prepn and use The beta-diketo acid dimer compound is prepared through coupling 4-aryl-4-oxy-2-hydroxy-2-butenic acid and diamine in different structure under the activation of coupling reagent to obtain diketo acid diamide, or reacting toluene dibromide and 3-hydroxy acetophenone under alkali condition to obtain benzyloxy radical connected diphenyl ethyl ketone; oxalylation and hydrolysis to obtain corresponding diaryl beta-diketo acid dimer. Pharmacological experiment shows that the compound of the present invention has very high HIV-1 integrase inhibiting activity.
US20100112056 Immediate release dosage forms of sodium oxybate The present invention provides a pharmaceutical composition, presented as a solid unit dosage form adapted for oral administration of sodium oxybate. The preferred unit dosage form is a tablet comprising a relatively high weight-percentage of sodium oxybate, in combination with a relatively small weight-percentage of total excipients. This permits the tablets to contain/deliver a pharmaceutically effective amount, e.g., about 0.5-1.5 g of sodium oxybate in each tablet with a delivery profile similar to that of the liquid form. The tablets are bioequivalent to the liquid form.
US7041241 Microspheres contain 5-fluorouracil coated with poly(d-l-lactic acid-co-glycolic acid); implanted in walls of operation site following exeresis of tumor, by intratissular injection The invention relates to the use of biodegradable microspheres that release a radiosensitizing anticancer agent for producing a medicament to be used simultaneously with, separately from or spread over time with a radiotherapy, for treating glioblastoma. The use of said biodegradable microspheres according to the invention results in a patient survival time of at least 90 weeks, a therapeutically effective concentration being maintained in the parenchymatous area throughout this time. The microspheres used preferably contain 5-fluorouracile of the tumor, by intratissular injection. The radiotherapy targeting the tumorous mass is dosed at 60 Gy over approximately 6 weeks. The invention also relates to a method for producing the biodegradable microspheres by emulsion-extraction, and to a suspension containing the biodegradable microspheres obtained using this method.
WO2013037390A1 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4 and R5 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
WO2010055006A1 Naphthylacetic acids used as crth2 antagonists or partial agonists The invention is concerned with the compounds of formula I and pharmaceutically acceptable salts and esters thereof, wherein X, Q and R1 -R3 are defined in the detailed description and claims. The invention is also concerned with the compounds of formula Z and pharmaceutically acceptable salts and esters thereof, wherein R1-R3 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I and Z as well as pharmaceutical compositions containing such compounds. The compounds of formula I and Z are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
US20080207543 Modified pituitary gland development in offspring from expectant mother animals treated with growth hormone releasing hormone therapy The intramuscular electroporated injection of a protease-resistant growth hormone-releasing hormone (“GHRH”) cDNA into rat dams at 16 days of gestation resulted in the enhanced long-term growth of the FI offspring. The offspring were significantly heavier by one week of age and the difference was sustained to 10 weeks of age. Consistent with their augmented growth, plasma IGF-I concentration of the FI progeny was increased significantly. The pituitary gland of the offspring was significantly heavier, and contained an increased number of somatotropes (cells producing GH) and lactotrophs (prolactin-secreting cells), and is indicative of an alteration in cell lineages. These unique findings demonstrate that enhanced GHRH expression in pregnant dams can result in intergenerational growth promotion, by altering development of the pituitary gland in the offspring.
US20120214820 Orally disintegrating pharmaceutical dosage form containing aripiprazole The present invention relates to an orally disintegrating dosage form containing aripiprazole. The formulation of the invention shows a fast disintegration.
CN101983650A Medicament for treating dermatitis aestivale The invention relates to a medicament for treating dermatitis aestivale. The component proportion of the medicament is as follows: phellodendron 6g, rhizoma atractylodis 6g, catnip 6g, common cnidium fruit 9g, windproof 6g and alum 3g. The accuracy of the ratio of the fixed dosages is plus or minus 10% of the above components. The medicament has the advantages of relieving itching, heat-clearing and detoxifying. The above medicament has an obvious and safe effect on treating dermatitis aestivale and is free of any toxic or side effect.
US20120108493 Polypeptide Fragments Comprising Endonuclease Activity and Their Use The present invention relates to polypeptide fragments comprising an amino-terminal fragment of the PA subunit of a viral RNA-dependent RNA polymerase or variants thereof possessing endonuclease activity, wherein said PA subunit is from a virus belonging to the Orthomyxoviridae family. This invention also relates to (i) crystals of the polypeptide fragments which are suitable for structure determination of said polypeptide fragments using X-ray crystallography and (ii) computational methods using the structural coordinates of said polypeptide to screen for and design compounds that modulate, preferably inhibit the endonucleolytically active site within the polypeptide fragment. In addition, this invention relates to methods identifying compounds that bind to the PA polypeptide fragments possessing endonuclease activity and preferably inhibit said endonucleolytic activity, preferably in a high throughput setting. This invention also relates to compounds and pharmaceutical compositions comprising the identified compounds for the treatment of disease conditions due to viral infections caused by viruses of the Orthomyxoviridae family.
CN101837024A Quick-acting medicament for curing tic disorder disease The invention relates to a quick-acting medicament for curing a tic disorder disease. The medicament is mainly prepared from the following raw material medicaments in part by weight: 10 to 50 parts of scorpion and 1 to 3 parts of borneol. The medicament is mainly prepared from the following raw material medicaments in part by weight: 27 parts of scorpion and 2 parts of borneol. The invention also provides application of the quick-acting medicament for curing the tic disorder disease in preparing medicaments for preventing and curing acute exacerbation of the tic disorder disease. The quick-acting medicament for curing the tic disorder disease can quickly control involuntary behaviors of patients, and experiments show that the effecting time of a quick-acting wind dispelling and action stopping No. 1 formula and a quick-acting No. 2 formula is about 5 minutes.
WO2008057604A9 Small molecule therapeutics, syntheses of analogues and derivatives and methods of use Provided herein are compounds that are inducers of apoptosis and activators of caspases and pharmaceutically acceptable derivatives thereof. Also provided are methods of synthesis of the compounds and methods for treatment of diseases in which there is uncontrolled cell growth and spread of abnormal cells, such as cancers, by administering the compounds.
CA2315818C Water-soluble eye drop Disclosed is a water-soluble eye drop comprising (a) at least one selected form carteolol and an acid addition salt thereof, (b) at least one acrylic polymer selected from a straight-chain type polyacrylic acid and a pharmaceutically acceptable water-soluble salt thereof, and (c) at least one selected from a water-soluble alkali metal salt and a water-soluble amine. The water-soluble eye drop of the present invention has a remarkably long duration time of drug efficacy, and is superior in intraocular pressure inhibition action and is effective for treatment of glaucoma.
US20110123586 Inhibition of quorum sensing-mediated processes in bacteria Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
US20080132484 Screening for a modulator of Polio Like Kinase, designing and identifying small molecule inhibitors using a homology model for PLK The present invention relates to a homology model for PLK, and the use thereof in assays for the identification of small molecule PLK modulators. The invention further relates to PLK modulators identified by said assays, and their use in the treatment of PLK-related disorders such as proliferative disorders.
CN103566375A Lansoprazole composition lyophilized powder injection The invention provides a lansoprazole composition lyophilized powder injection, and relates to the technical fields of medicines and medicine manufacture. The injection comprises the following raw material components in parts by weight: 1.75-2.14 parts of lansoprazole, 0.87-1.07 parts of chitosan nano-particles, and 96.80-97.38 parts of injection water. The lansoprazole composition lyophilized powder injection has the advantages that the composition composed of lansoprazole and chitosan nano-particles in a ratio of 1:0.5 can remarkably prolong the half life of a medicine, the acting time of the medicine can be prolonged, the bioavailability of the medicine can be increased, and the times that a patient takes the medicine can be reduced; an in vitro experiment investigates the stability of the lansoprazole composition lyophilized preparation in tests on influencing factors, acceleration tests and room temperature sample-reserving tests, and the result proves that the stability of a lansoprazole composition lyophilized preparation is more stable than that of injection lansoprazole with single component. Mice and rabbits are used as tested objects to observe the safety of a lansoprazole lyophilized lipidosome injection, and the result indicates that the injection lansoprazole composition does not have irritation, pyrogen or hemolysis, and can meet the requirement of intravenous injection.
EP2712865A1 Improved process for the preparation of ambrisentan The invention relates to improved processes for the preparation of ambrisentan. The invention also relates to new polymorphic form of ambrisentan. In particular, it relates to a polymorphic form, designated as Form I of ambrisentan and a process for the preparation of the Form I.
CN103127306A Footbath liquid preparation method The invention discloses a footbath liquid preparation method, which provides a footbath liquid for preventing beriberi and having health care effect. A technical scheme is characterized in that that Artemisia argyi, ground tea and salicylic acid are employed to prepare the footbath liquid. The preparation method comprises the following steps: 1) air dried Artemisia argyi and ground tea are placed in a drug decorating pot, cold water is added for boiling by slow fire to obtain an Artemisia argyi tea soup; 2)Artemisia argyi tea dreg can be filtered to obtain an Artemisia argyi tea decoction; 3)the Artemisia argyi tea decoction is cooled; 4) a salicylic acid solution is added in the cooled Artemisia argyi tea decoction to obtain the footbath liquid; and 5)the footbath liquid enables vacuum package. The adopted technical scheme has convenient operation, the smell of the footbath liquid is fragrant, and the footbath liquid has the effects for preventing and treating beriberi and foot health care effect.
US20080213236 Natural Remedy-Dietary Supplement Combination Product A natural remedy-dietary supplement combination product which comprises omega-3 fatty acids, α-tocopherol, ascorbic acid, selenium, Harpagophytum procumbens (devil's claw) and Boswellia serrata or carterii (frankincense), with the proviso that it does not comprise a plant or plant extract of the Saxifragaceae family, and a method of treating a chronic inflammatory disorder and/or a rheumatic disorder.
EP2111858A1 Novel treatment for alzheimer's disease The present invention concerns a new pharmaceutical composition comprising an antagonist and a co-agonist of the N-methyl-D-aspartate-type glutamate receptor (NMDAR). The inventors found that the co-administration of these two compounds effectively inhibits production of amyloide-β peptide. In patient's suffering from Alzheimer's disease, these peptides are deposited in the extracellular matrix forming neuritic "plaques". Therefore, the present inventors identified a new possibility for prophylaxis and/or treatment of Alzheimer's disease by stopping the continued formation of neuropathological extracellular deposits.
WO2013170115A1 Pyridazine and pyridine derivatives as nampt inhibitors Disclosed are compounds of formula (IC), or a therapeutically acceptable salt thereof which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
CN1977905A Rose oral liquid and its preparing method The present invention relates to an-oral liquor with the functions of improving one's looks and beautifying one's face. In the concrete, it relates to a rose oral liquor and its preparation method. Its composition includes (by wt%) 2-10% of honey, 0.05-0.3% of vitamin and the rest is fresh rose flower extract. Its preparation method includes the following steps: adding rose flower extract into a stirrer, heating to 50-70 deg.C, adding honey, stirring them, cooling to 25-35 deg.C, adding vitamin, stirring them, cooling and filtering so as to obtain the invented finished product.
US20100173856 Methods of producing and using nutritional and pharmaceutical compositions that include one or more active substances Methods for producing a composition that includes an active agent, nutraceutical and pharmaceuticals compositions, and methods for ameliorating and/or treating a disease using the composition that includes an active substance are described herein. More particularly, methods for producing a composition that contains one or more active substances such as oleocanthal, pharmaceutical compositions that include one or more active substances such as oleocanthal, and methods of ameliorating and/or treating inflammation using compositions that contains one or more active substances such as oleocanthal are described.
CN103230535A Medicinal liquor with function of activating collaterals to ease pain The invention discloses medicinal liquor with the function of activating collaterals to ease pain. The medicinal liquor is prepared from the following raw materials: 50g of disporopsis fuscopicta, 50g of aconitum anthora, 50g of sinense knotweed rhizome, 50g of sanqi, 50g of rhizoma panacis majoris, 50g of sedum uizoon, 50g of radix caulophylli, 100g of radix rehmanniae, 40g of safflower, 40g of draconis resin, 2g of musk, 100g of camphor, 80g of borneol, 60g of menthol, 1000ml of 95% of alcohol and 10kg of white spirit. The medicinal liquor has the functions of relaxing muscles and stimulating blood circulation, eliminating swelling and removing stasis, clearing channels and collaterals and expelling wind-damp, can timely relieve pains, can be used for treating various new and old soft tissue injuries, cervical spondylosis, lumbar spondylosis, arthritis, cold-dampness Bi syndromes, fractures in later stage and the like and has obvious curative effects.
US20120065200 Inhibitors of notum pectinacetylesterase and methods of their use Compounds are disclosed for the treatment, management and prevention of diseases and disorders affecting the bone. Particular compounds are potent inhibitors of Notum Pectinacetylesterase, and are of the formula: wherein E, G, Y, Z, R1, R2, and R3 are defined herein.
US7468357 Nucleosides with anti-hepatitis B virus activity A method for the treatment of a host, and in particular, a human, infected with hepatitis B virus (HBV) is provided that includes administering an effective amount of a β-L-nucleotide, optionally in combination therapy with other drugs for the treatment of HBV or human immuno-deficiency virus (HIV).
WO2012042482A1 Process for the synthesis of funicone analogues The present invention relates to the synthesis of analogous compounds of funicone, some of which are not found in nature, which comprises the preparation of compounds having general formula (III) and (IV) and the subsequent coupling reaction of said compounds in dimethylformamide by means of carbon monoxide in the presence of palladium allyl chloride dimer, to obtain compounds having formula (V) (scheme 2).
US20100120702 Solid preparation for dialysis The present invention provides a glucose decomposition-suppressed solid preparation for dialysis among powdery or granular preparations for dialysis containing acetate-free solid organic acids as pH adjusting agents. The present invention provides the solid preparation for dialysis containing electrolytes, glucose and pH adjusting agents characterized in that solid organic acids containing reduced amount of microparticles are used, and more specifically, characterized in that solid organic acids whose 20 or less percent of particles are 250 μm or less in diameter, or solid organic acids whose 10 or less percent of particles are 150 μm or less in diameter, are used. Preferably, the solid organic acid contained therein is citric acid.
EP2784076A1 Dimeric SMAC mimetics The invention provides small molecule mimics (IV) of the Smac peptide that are dimers or dimer-like compounds having two binding domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
CN102949332A Oral anti-depression slow-release and controlled-release medicinal composition containing citalopram The present invention provides a new technology of slow-release and controlled-release preparations for SSRI anti-depressant drugs. With the present invention, in the foreseeable clinical administration way, the number of administration can be effectively reduced, a blood drug level can be effective stabilized, medicine taking compliance of patients can be substantially improved, and side effects can be reduced well.
EP2018185A1 Use of mas-g-protein-coupled receptor agonists in the treatment of the metabolic syndrome, its components and its complications The present invention is characterized by the use of Mas-G- protein-coupled receptor agonists for the control, prevention and treatment of the body levels of triglycerides, cholesterol and glucose, as well as of hyper- tension and possible increase in body weight, which are characteristic of the clinical manifestation of the metabolic syndrome and its complications. Another characteristic of the invention is the use of Mas-G-protein- coupled receptor agonists, including the Angiotensin-(1-7) peptide and its analogs, agonists, either peptidic or non-peptidic, as modulators of the mani- festations of insulin resistance and glucose intolerance and in the prevention and treatment of the related alterations. The invention claims the use of MAS-G-protein-coupled receptor agonists, formulated with pharmaceutically and pharmacologically acceptable excipients or carriers, and Mas-G-protein-coupled receptor agonists, includ- ing the Angiotensin-(1-7) peptide and its analogs, agonists, either peptidic or non-peptidic, as modulators of the metabolic syndrome, the diseases that compose it and its complications.
US20060241126 Phospholipase inhibitors perticularly phospholipase A2 enzyme Lipoprotein Associated Phospholipase A2; N-(1-Methylpiperidin-4-yl)-(2-(2-(2,3-difluorophenyl)ethyl)-4-oxo-4H-pyrido[2,3-d]pyrimidin-1-yl)-N-(4-(4-trifluoromethylphenyl)phenyl)methylacetamide; amidation Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
CN101884636A Application of corosolic acid in preparation of antineoplastic medicine The invention relates to the technical field of medicine, in particular to the application of corosolic acid in preparation of antineoplastic medicine; and when being combined with pharmaceutically acceptable supplementary material, the corosolic acid can be prepared into various oral, injection and external preparations and has better development and application prospect. On the basis of discovering that the corosolic acid has stronger antineoplastic action, the inventor further explains the mechanism of the antineoplastic action of the corosolic acid, thus retarding cancer cells at S period and inducing cell apoptosis mediation.
CN102106808A Solid preparation and preparation method thereof The invention discloses a method for preparing a solid risperidone preparation. The method comprises the following steps of: dissolving risperidone into acid solution containing an acidulant to obtain medicament-containing acid solution; and uniformly mixing excipients and the medicament-containing acid solution, and performing wet granulation. The invention also discloses the solid risperidone preparation prepared by the method. The method overcomes the disadvantages of serious pollution, high loss and serious potential safety hazards caused by mechanical pulverization treatment, is convenient and easy to operate, has high safety factor, and is easily applied to industrialized production. The solid risperidone preparation prepared by the method has excellent dissolution characteristic, stability and content uniformity.
WO2007058601A1 Novel 2-amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cognitive impairment, alzheimer’s disease, neurodegeneration and dementia This invention relates to novel compounds having the structural formula I below and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
US20130059821 Bicyclic aryl sphingosine 1-phosphate analogs Compounds that have agonist activity at one or more of the SIP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SIP receptors.
WO2010084121A1 Novel diaza-bicyclononyl-pyrimidinyl derivatives and their medical use This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyhmidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
CN102688247A Application of nestorone to preparation of drugs for treating Parkinson's disease The invention provides application of nestorone (16-methylene-17alpha-acetyloxy-19-norpregn-4-ene-3, 20-dione, nes) to preparation of neuroprotective drugs for improving and treating Parkinson's disease. The prepared drugs contain preparation-allowable drug excipients or carriers. The drugs can be made into the forms of liquid, particle, controlled release formulation, electuary, tablet or capsule. In terms of cells, the neuroprotective drugs and application thereof using nestorone to improve and treat Parkinson's disease are demonstrated, and the curative effect of the neuroprotective drugs compared with progesterone on improving and treating Parkinson's disease is better, and the toxic and side effects to nervous systems are low.
US7196096 Substituted amines of spirofuropyridines useful in therapy Methods for the treatment of psychotic or intellectual impairment disorders with compounds of formula I, wherein A, R and R1 are as defined in the specification.
CN101380349B Specific ointment for burn and scald The invention relates to a formula of an ointment for burns and scalds and a preparation method thereof. The formula comprises: 2-12 percent by weight of borneol, 3.5-12.5 percent by weight of frankincense, 2.5-11.5 percent by weight of myrrh, 25-36 percent by weight of vaseline, 1-12.5 percent by weight of red lead, 3-18 of percent calcined gypsum, 10-30 percent by weight of sesame oil, appropriate amount of beeswax, appropriate amount of lithargite and appropriate amount of boric acid. The formula is applicable to the first-degree, the second-degree and the small area third-degree wounds and can also be used for the wounds of small area skin defects. The invention provides the ointment for the burns and scalds with anti-infection, no pains, fast healing, no scars and convenient use, thereby replacing the skin grafting with great risk, high cost and great suffering of patients. The preparation method comprises the steps as follows: 1. the drugs are ground and finely screened; 2. the drugs are sequentially added and dissolved according to the features of the drugs; 3. the sterilization, the cooling and the filling are carried out.
WO2008000669A1 Improving tolerance to anti-inflammatories The invention relates to the use and composition of pharmaceutical formulations comprising non-steroidal anti-inflammatory drugs. Different types of magnesium citrate salts are used as an additive at an adequate dose ratio in order to improve cellular tolerance to non-steroidal anti-inflammatory drugs.
US20080248093 pH sensitive prodrugs of 2,6-diisopropylphenol The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
US20120058099 Use of hypoxanthine for promotion of neuronal outgrowth Disclosed herein is a method of promoting neuronal outgrowth in a neuron. The method comprises contacting the neuron with an effective amount of hypoxanthine, to thereby promote neuronal outgrowth of the neuron. The hypoxanthine may be contacted in the absence of xanthine oxidase and/or in the absence of exogenous nerve growth factor (NGF), and/or in the absence of exogenous D-mannose, and/or in the absence of exogenous oncomodulin, and/or in the absence of exogenous TGF-B. The neuron may be an optic nerve neuron or a retinal neuron and/or an injured neuron. Neurons may be from the central nervous system (CNS) or the peripheral nervous system (PNS). The methods are useful for treating an injured neuron, for example to an optic nerve neuron, resulting from branch and central vein/artery occlusion, trauma, edema, angle-closure glaucoma, open-angle glaucoma. Methods of treatment of various neurological injuries and diseases, as well as therapeutic compositions, are also disclosed.
CN102040585A Selective estrogen receptor regulator The invention relates to a compound which can be used as a selective estrogen receptor regulator. Compared with the traditional selective estrogen receptor regulator, the compound has reduced oxidative metabolism, higher water solubility and effective bioavailability, and therefore, the compound has the advantages of lower dosage and small side effect. As a ligand of an estrogen receptor, the compound can be used for treating or preventing various indications which are related to estrogen functions, and especially, the compound can be used for treating postmenopausal breast cancer osteoporosis.
CN1911209A Quick-disintegration tablets of calcium atovastatine, and its prepn. method A fast disintegrated atorvastin calcium tablet is prepared from atorvastin calcium, disintegrant, flavouring, filler and lubricant proportionally. Its preparing process is also disclosed.
CN102552305A Drug for treating pig high-fever high-temperature diseases The invention discloses a drug for treating pig high-fever high-temperature diseases, which comprises the following raw materials according to the proportional ratio by weight: 10 g of ampicillin sodium injection, 1000 units of coenzyme A injection, 100 ml of inosine injection, 1000 g of terramycin, 1000 particles of chloromycetin and 500 g of high-energy electrolytic multivitamins. The drug has the advantages that high fever and high temperature caused by various bacteria and viral infection soft tissues based on high-fever diseases, skin drying, red turning, purple turning and other multiple diseases, fibrous bleeding of livers, kidneys, spleens, stomachs, intestinal tracts and the like, and lymph gland atrophic saliva are reasonably and scientifically mediated and treated.
US20090087481 Using mixture comprising colony stimulating factor, interleukin-5 and/or a mimetic as therapeutic tool in treatment of nervous system disorders The present invention relates to a method of treating a neurological condition in a mammal by administering at least one hematopoietic growth factor.
EP2530068A1 New strontium salts, synthesis and use thereof in the treatment of osteoporosis The present invention relates to a strontium salt (I) wherein n is an integer which can take the values of 0 or 1 m is an integer which can take the values of 0 or 1 R is hydrogen, methyl or ethyl and stereoisomers or hydrates thereof, to methods for its synthesis, and use in the treatment and/or prophylaxis of a cartilage and/or bone disease and/or conditions resulting in a dysregulation of cartilage and/or bone metabolism in a mammal.
WO2008081928A1 Pyrazolopyrimidine compound Disclosed is a novel compound having Syk and/or Abl inhibitory activities, which is useful for prevention/treatment of allergic diseases, autoimmune diseases, arthritides and cancers. Specifically disclosed is a pyrazolopyrimidine compound represented by the formula [I] or [III] below, a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a solvate of any of them.
CN102504989A Male health wine The invention relates to a male health wine, and is characterized in that the male health wine comprises the following raw materials by weight: ginsenoside 0.05 kg, male silkworm moth 2.5 kg, red ant 0.5 kg, longspur epimedium 0.8 kg, shizandra berry 0.4 kg, penis cervi 0.075 kg, penis canitis 0.3 kg, pizzle 0.27 kg, eucommia bark 0.5 kg, actinolite 0.04 kg, and aweto 0.1 kg; all the raw materials are cleaned out to remove impurities, and then mixed with 38 to 45 DEG alcohol or the edible wine base of a pure grain wine under the ordinary temperature; liquid and solid in the mixture are directly separated with each other after being placed in a reaction kettle for 35 minutes under the conventional pressure of 0.2 Pa; the separated liquid is taken for blending and brewing; white granulated sugar 0.25 kg is added according to different taste; and clarification is carried out after blending. The male health wine is mainly used for conditioning yin-yang qi and blood of a human body by mainly entering a kidney and a spleen, activating functions of five organs to regulate immunity, and delaying aging, can be added into a daily diet trophic structure, facilitates nourishing, takes effect fast without long-term wait, and is a superior health-care product integrating the effects of nourishing and curing.
US7335674 Benzothiazole-4,7-diones and benzoxazole-4,7-diones with substituents in position 5 or 6 and method for production thereof A targetted production method for benzothiazole-4,7-dione and benzoxazole-4,7-dione derivatives, mono-substituted in the 5 or 6 position with an amino group, itself optionally substituted.
CN102100688A Application of zedoary cyclic diolefine in preparation of medicine for resisting neoplasm metastasis The invention belongs to the field of pharmacy, and provides application of zedoary cyclic diolefine in preparation of a medicine for resisting neoplasm metastasis, and in particular relates to application in the preparation of medicines for resisting neoplasm metastasis, such as liver cancer, gastric cancer, carcinoma of urinary bladder, breast cancer, colon cancer, kidney cancer, esophagus cancer, gallbladder cancer, ovarian cancer, pancreatic cancer, carcinoma of uterine cervix, thyroid cancer, prostatic cancer, oral cancer, lung cancer and the like. The zedoary cyclic diolefine plays a role in resisting the neoplasm metastasis through inhibiting the expression of proteins related to neoplasm cell metastasis.
WO2010015586A2 2,3,4,7-tetrahydro-indolo[2,3-c]quinoline compounds The present invention pertains to 2,3,4,7-tetrahydro-indolo[2,3-c]quinoline compounds, as well as the resulting pharmaceutical compositions, and their use in the treatment or prophylaxis of diseases alleviated by inhibition of type 5 phosphodiesterases. Furthermore, the present invention pertains to the methods of manufacturing these 2,3,4,7-tetrahydro-indolo[2,3-c]quinoline compounds.
CN101642433B Nimesulide liposome solid preparation and preparation method of drug composite thereof The invention provides a Nimesulide liposome solid preparation and a preparation method of the drug composite thereof. For the Nimesulide liposome solid preparation of the invention, the active ingredient Nimesulide is prepared into liposome and then prepared into Nimesulide solid preparation with other ingredients, wherein the liposome is prepared by the following ingredients according to parts by weight: 1 part of Nimesulide, 3-10 parts of lauric acid glycerol monolaurate, 0.5-4 parts of cholesterol, and 0.1-2 parts of poloxamer188. Compared with the existing Nimesulide liposome solid preparation, the Nimesulide of the invention has high dissolution rate and improved bioavailability, and overcomes the detect that the bioavailability of the Nimesulide liposome solid preparation in the prior art is low.
WO2012130299A1 Peptidase inhibitors Novel compounds of the formula (I) wherein R1, R2, D, A, B and X have the meanings defined herein, pharmaceutical compositions comprising them as active ingredient, as well as their use in medicine, in particular as peptidase inhibitors, more specifically inhibitors of cysteine and/or serine peptidases useful in the treatment/prevention of inflammatory diseases.
CN103230002A DHA (docosahexaenoic acid) liposome preparation method The invention discloses a DHA (docosahexaenoic acid) liposome preparation method. By taking fat-soluble DHA as a raw material, taking lecithin and cholesterol as membrane materials and combining the traditional membrane method and a novel dynamic high-pressure method, the method comprises the following steps: dissolving, evenly mixing, performing reduced pressure evaporation, and performing dynamic high-pressure treatment and other treatment operations to prepare DHA liposome. The DHA encapsulation rate of the liposome is 50-70%; the average particle size is 80-160nm; and the product has favorable storage stability.
CN101959883A 3-indazolyl-4-pyridylisothiazoles The present invention provides 3-indazoyl-4-pyridylisotbiazoles of the following formula or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and methods of using the same, as well as processes for preparing the same, and intermediates thereof.
WO2009022009A1 Pharmaceutical composition comprising a pyrazole-o-glucoside derivative The invention relates to a pharmaceutical composition according to claim 1 comprising a pyrazole-O-glucoside derivative in combination with a DPP IV inhibitor which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
WO2011030104A1 Phenylacetate and/or phenylbutyrate (not ornithine) for reducing portal blood pressure The present invention provides a method of reducing portal blood pressure comprising administering to a subject in need thereof a formulation comprising phenylacetate and/or phenylbutyrate, wherein the formulation does not comprise ornithine.
US20120244141 Stratification of cancer patients for susceptibility to therapy with PTK2 inhibitors A method for determining whether a cancer patient is susceptible to treatment with a protein tyrosine kinase 2 (PTK2) inhibitor, comprising detecting the expression of the E-cadherin protein in a cancer sample of said cancer patient, wherein an E-cadherin protein immunoreactivity score (IRS) of 0-2 indicates that the cancer patient is susceptible to treatment with a PTK2 inhibitor. The invention further encompasses treatment of a patient with a protein tyrosine kinase 2 (PTK2) inhibitor if it has been so determined that said patient is susceptible to such treatment.
CN202409448U Anorectum fumigator The utility model discloses an anorectum fumigator comprising a case, a liquid medicine liner, a controller, a heating wire and a power line. The anorectum fumigator is characterized in that the liquid medicine liner is arranged in the case, the heating wire is arranged on the bottom of the liquid medicine liner and connected with the power line, and a controller arranged on the case is used for controlling temperatures. The anorectum fumigator is rational in structure and convenient to use and has a very good effect on the prevention and cure of anorectum diseases.
CN101928321A Acidic amino acid chemically-modified ursolic acid derivatives with anti-cancer activities The invention relates to a series of acidic amino acid chemically-modified ursolic acid derivatives with anti-cancer activities. Ursolic acid used as parent compound is bonded with acidic amino acid to obtain the ursolic acid derivatives. The in-vitro pharmacological test indicates that the acidic amino acid chemically-modified ursolic acid derivatives with anti-cancer activities have obvious in-vitro inhibition capacity for human liver cancer HepG2, human colon cancer HT-29, human stomach cancer AGS and human neuroblastoma SH-SY5Y.
US20100240754 Unsaturated fatty amino acid derivatives and use thereof in dermal cosmetology The present invention relates to drugs consisting of unsaturated fatty amino-acid derivatives of the general formula (I), and to their pharmaceutically acceptable acid addition salts, in which: X is oxygen or NH, Rn are independently hydrogen or a (C1-C6)alkyl optionally substituted by halogen; R1 is hydrogen, fluorine, chlorine or bromine, or a CF3 or CHF2 or a (C1-C6)alkyl, (C1-C6)alkenyl or (C1-C6)alkynyl, optionally substituted by one or more halogen atoms; R is hydrogen or a (C1-C6)alkyl or (C3-C6)cycloalkyl optionally substituted by one or more halogen atoms; Ra and Rb are independently hydrogen (C1-C6)alkyl or (C1-C6)acyl, and Ra and Rb a hydrocarbonated cycle containing 4 to 6 carbon atoms; and n is an integer between 2 and 14.
CN1743330A Aspergillus fumigatus dardarin C analogue, and its synthesizing method and use This invention discloses a new series of Aspergillus fumigatus tremorine C-likes and their preparation method and its use in medicine field. The preparation method is as follow: first, with base as catalyst, the 2-position functional groups in (1S/R, 3S)-(2, 2-dimethoxy ethyl)- 1, 2, 3, 4-tetrahydro-beta-carboline-3-carbomethoxylate are acylated by activated Fmoc-Pro-OH; then, with the presence of base catalyst, at the same time of Fmoc removal, the acylates are intramolecularly cyclized; next, after the cyclized resultants are hydrolyzed and deacetalized by heating under acid catalysis, the resultants react with amino acid methyl ester hydrochlorides to be dehydrated and condensed under base catalysis, then reduced buy reducer, and finally the reduction product is saponified under base catalysis. As shown in experiment this compound has higher anti-tumor activity.
CN1634011A Ibuprofen gelling preparation and its preparation method The invention relates to an ibuprofen gelling preparation and its preparation method which is a gel form oral administration preparation prepared through using ibuprofen and right amount of base material as gel or paste, compared with the prior arts, because the preparation is made into the form of jelly or paste form gel, the aged people and children are willing to take the preparation, thus overcoming the inconvenience of medicine-taking. The invention realizes fine therapeutic action, and the functions of antiphlogistic, analgesic and analgesic.
WO2010092436A1 Pharmaceutical combinations of simethicone and otilonium This invention relates to pharmaceutical combinations, compositions and kits of simethicone and otilonium bromide and methods of using such combinations to treat patients suffering from irritable bowel syndrome (IBS) and/or pain and spasm of the distal enteric tract and/or painful symptoms of too much gas in the gastrointestinal tract.
CN103751117A Carvedilol sustained-release capsule The invention relates to the field of pharmaceutical preparations, in particular to a carvedilol sustained-release capsule. The carvedilol sustained-release capsule is characterized by consisting of a drug-containing pill core and a sustained-release layer, wherein the drug-containing pill core contains a blank pill core and carvedilol; the sustained-release layer contains a film-forming material and a pore-forming agent; the drug-containing pill core also contains a solubilizer; a weight ratio of the solubilizer to the active ingredients is (1:8)-(3:8); the sustained-release layer accounts for 12.6-16.1 percent of the total weight of the micro pill; the pore-forming agent consists of a methacrylic acid-ethyl acrylate (1:1) copolymer and a methacrylic acid-ethyl acrylate (1:2) copolymer; the pore-forming agent accounts for 6-11 percent of the total weight of the sustained-release layer. According to the carvedilol sustained-release preparation, only a micro pill is needed to be prepared, and a sustained-release effect can be achieved. Moreover, the medicine is slowly and fully released in main absorption parts at the pH of 5.5-6.8, the drug action time is prolonged, and the phenomenon that the safety risk of a patient is increased due to the local drug overdose caused by drug short-rate pulse release is avoided.
WO2009153897A1 Stemonamide synthesis intermediate and pharmaceutical composition for prevention and/or treatment of cancer Disclosed is a compound which is effective for prevention and/or treatment of cancers. Specifically disclosed is a compound represented by the formula (I) below, or a salt, solvate or physiologically functional derivative thereof. Also disclosed is a composition for prevention and/or treatment of cancers, which contains such a compound, or a salt, solvate or physiologically functional derivative thereof, as an active ingredient. (In the formula, R1-R6, x and y are as defined in the description.)
WO2011053508A1 ALKYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS This invention relates to a novel arylindenopyrimidinc, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. (Formula), wherein X, R2, R3, and R4 are as defined in the specification.
US7419974 Cyclohexyl(alkyl)propanolamines, preparation method and pharmaceutical compositions containing same The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen atom, a (C1-C6)alkyl group, a (C1-C4)alkoxy group, a —COO(C1-C4)alkyl group, a —CO(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl groups, —NO2, —CN, —CONR4R5, —COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; R4 and R5 represent, independently, a hydrogen atom, a phenyl, a (C1-C4)alkyl group or a phenyl-(C1-C4)alkyl group or R4 and R5 with the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.
WO2009129181A1 Propanediol-dicarbamate derivatives This disclosure relates to novel propanediol-dicarbamates, their derivatives, pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual N-methyl D-aspartic acid (NMDA) receptor antagonist and sodium channel blocker.
US20130059818 Carbosilane dendrimers and the use thereof as antiviral agents Highly branched macromolecules synthesized from a polyfunctional core, preferably silicon, or polyphenolic, with a carbosilane structure at its periphery functionalized with groups, preferably anionic, giving to the macromolecule a net negative charge. Furthermore, the invention relates to the procedures for their synthesis and their uses as antiviral agents, antibacterial and antifungal agents.
EP1758874A1 Substituted thiazoleacetic acids as crth2 ligands Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is -S-, -O-, -N=N-. -NR7-, -CR7=CR8-, -CR7=N-, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group -COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.
CN102451186A Preparation method of cinnabar powder The invention relates to a preparation method of cinnabar powder, which comprises the following steps: purifying cinnabar ore, soaking in water, taking the soaked cinnabar out, grinding with water, injecting the slurry formed after grinding into a separator from the side parts with fine cinnabar powder suspending in the upper layer of the slurry, performing centrifugation, continuing grinding the crude cinnabar powder, cycling the above steps till the fineness of all the cinnabar powder reaches above 200 meshes; performing solid-liquid separation of slurry with cinnabar powder fineness of above 200 meshes to obtain a cinnabar powder wet block, drying at a temperature of 20-40 DEG C, grinding by a grinder to allow the cinnabar powder to be in a dispersing state, performing vacuum packaging. The method of the invention has strong operationality, is suitable for continuous production, greatly increases the production efficiency, reduces the production cost to a certain extent, and has very good popularization application value.
US20100068203 17-Oxymacbecin Derivatives and Their Use in the Treatment of Cancer and/or B-Cell Malignancies The present invention relates to 17-oxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.
CN102875576A Synthesis of antibiotic ceftazidime, ceftazidime for injection and preparation method of ceftazidime The invention discloses synthesis of antibiotic ceftazidime, ceftazidime for injection and a preparation method of ceftazidime. 7-ACA is served as a raw material, silanization and iodo reaction are carried out, and pyridine, hydrochloric acid and water are added to obtain TA (7-PyCA); ceftazidime active ester is added in an organic solvent and an inorganic solvent to obtain new modified ceftazidime active ester; TA is added in new modified ceftazidime active ester, organic mixed solvent and triethylamine are added, then acid water and an acetone solution are added to obtain TC (ceftazidime dihydrochloride), and ceftazidime is obtained through the reaction. The synthesis of ceftazidime provided by the invention has the advantages that ceftazidime is high in yield, operation processes are simplified, production cost is low, ceftazidime is applicable to industrial production, obtained products can be stored for a long time, a structure is stable, and impurity content is low. Ceftazidime for injection has the advantages of being moderate in grain size, good in clarity, less in impurity content, excellent in quality, stable and the like, and is high in split charging efficiency in production, good in content uniformity, high in medicine dissolution rate in clinical application and good in dissolubility.
US6989450 Aldol condensation of a ketonic compound containing free or protected alcohol group with a acid or or metallic salt group containing compound to form intermediate, performing macrolactonizing of the intermediate The present invention relates to methods for use in producing epothilones and analogs and derivatives thereof. A general method according to the present invention broadly comprises performing an aldol condensation of a first compound with a second compound thereby to form a third compound selected from the formulas: and stereoisomers thereof, and performing a macrolactonization of the third compound. The present invention also provides chemical compounds, and methods for producing such chemical compounds, that are useful in producing epothilones and analogs and derivatives thereof.
CN102920995A Drug composition for treating liver injury The present invention relates to a drug composition for treating liver injury. A technical scheme of the present invention is that the drug composition comprises, by weight, 1-200 parts of glycyrrhizin, 1-200 parts of L-cystyldi L-aspartic acid, and 1-200 parts of glycine. The drug composition has characteristics of stable property and good water solubility, and is easily made into a preparation.
CN101099755A Medicine for treating allergic rhinitis and cold rhinitis The present invention relates to a medicine for effectively and quickly curing the diseases of allergic rhinitis and coryzal rhinitis, etc. said medicine composition contains polyethylene glycol, domiphen bromide, chlorhexidine and brucea fruit extract. Its effective rate can be up to 100%.
WO2009059388A1 Use of antagonists of platelet receptor factor for the treatment of infections caused by the influenza virus The present invention refers to the receptor antagonists of the platelet activation factor (PAF), their analogues and/or derivatives for treating infections caused by the influenza virus.
EP1066038B1 Use of cabergoline in the treatment of restless legs syndrome The present invention provides for the use of cabergoline and other agents for the treatment of restless legs syndrome (RLS).
EP2100139A2 Biologically active compositions, methods for producing the same and biological applications Use of a product from plants comprising extracts, fractions and/or molecules as G-protein coupled receptor (TGR5) specific agonist, having minimum effective concentration (EC50) of greater/equal to TGR5 natural ligand comprising litocholic acid, not activate the farnesoid X receptor (FXR) nuclear receptor, inducing a reduction of weight gain induced by a fatty food to a model, who has metabolic syndrome, and a reduction of mass of fatty cell of epididymis in the models, and inducing a improvement of glucose tolerance, is claimed. Use of a product from plants comprising extracts, fractions and/or molecules as G-protein coupled receptor (TGR5) specific agonist, where the plant extract or fraction is obtained from the extract or the molecules is obtained by the extract or fractions, having minimum effective concentration (EC50) of greater or equal to TGR5 natural ligand, such as litocholic acid, not activate the farnesoid X receptor (FXR) nuclear receptor, inducing a reduction of weight gain induced by a fatty food to a model, who has metabolic syndrome, as well as a reduction of mass of fatty cell of epididymis in the models, and inducing a improvement of glucose tolerance, is claimed. - ACTIVITY : Metabolic; Anorectic; Antidiabetic. - MECHANISM OF ACTION : G-protein coupled receptor agonist. Tests details are described but no results given.
EP1721898A1 Quinoline and pyridoquinoxaline derivatives as antibacterial agents This invention relates to certain novel pyrido[2,3-f]quinoxaline-8-carboxylic acid derivatives, their isomeric pyrido[2,3-g]quinoxaline-carboxylic acid derivatives, corresponding 4-oxo-1,4-dihydroquinoline-3-carboxylate derivatives of formulas (A) and (B) and physiologically tolerated salts and esters thereof, a process for their preparation and their potential use as antibacterial compounds.
CN102796092A Oxazolidinone derivative, and preparation method and application thereof The invention relates to an oxazolidinone derivative, and a preparation method and application thereof. A group of substituted oxazolidinone compounds represented by a structure shown in a general formula belongs to the field of pharmaceutical chemistry. The invention specifically relates to the substituted oxazolidinone compound represented by a general formula I, wherein R1 represents chlorine, bromine, methyl or trifluoromethyl; and R2 represents a C1-10 straight or branched saturated or unsaturated alkylidene chain. The compound or medical salt thereof can be directly used as an Xa factor inhibitor and an anti-thrombotic agent, and is used for treating cardiovascular and cerebrovascular diseases and thromboembolism diseases.
CN101367811A Carbon substituted penems antibiotics The present invention belongs to the technical field of medicine, in particular to a carbapenem antibiotic with antibiotic activity shown in the formula (I) and a pharmaceutically acceptable salt, an easily hydrolyzed ester, a hydrate and a hydrate of the ester or the salt thereof: wherein, R<1>, R<2>, R<3>, R<4>, R<5> and R<6> are defined in the description. Moreover, the present invention also provides preparation methods of the compounds, drug combinations containing the compounds and applications of the compounds in the preparation of drugs for treating and/or preventing infective diseases.
CN103509014A Salts of antofine derivatives The invention relates to fumarates of antofine and antofine derivatives or pharmaceutically acceptable solvates thereof, and an application of the fumarates or the solvates in preparing drugs for treating cancers.
CN103239424A Metformin hydrochloride sustained-release capsule and its preparation method The invention relates to a metformin hydrochloride sustained-release capsule and its preparation method. The metformin hydrochloride sustained-release capsule is prepared by steps of coating a metformin hydrochloride granule sustained-release material and putting into an enteric capsule. In comparison with the prior art, sustained-release granules and enteric capsule filling technology are combined together to prepare the new dosage form of metformin hydrochloride sustained-release (enteric-coated) capsule. As the sustained-release granule coating and enteric capsule filing technology is adopted, metformin hydrochloride will not be disintegrated and will not stimulates gastric mucosa, and adverse reactions such as nausea, stomachache, diarrhoea and the like caused by medication can be avoided. Meanwhile, metformin hydrochloride will not be damaged by gastric juice, and bioavailability of metformin hydrochloride is raised. In addition, the product provided by the invention is also a sustained-release enteric-coated preparation. The medicine can be stably released in a body, effective plasma concentration is maintained for a long time, and toxic and side effect which might be caused by higher plasma concentration within a short time are avoided. The frequency for taking the medicine is reduced, and patient compliance is also raised.
WO2006090815A1 Agent for preventing development of prion disease, food additive and feed additive comprising the same There has been found no substantially effective method for treating/preventing prion diseases which are neurological diseases caused by impairment of central nervous system by prion (i.e., abnormal prion protein), including Creutzfeldt-Jakob disease (CJD), Gerstmann-Straussler-Scheinker syndrome (GSS), scrapie in animals, bovine spongiform encephalopathy (BSE) and chronic wasting disease (CWD). Then, it is intended to provide an agent for preventing the development of a prion disease, a food additive and a feed additive having inhibitory effect on the proliferation of abnormal prion protein by utilizing a natural food material ingested orally in daily life. The agent comprises fucoidan as an active ingredient. The food additive or feed additive comprises the agent.
EP2563765A1 Bicyclic compound derivatives and their use as acc inhibitors. The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.
CN101849902A Preparation method of solid pharmaceutical composition containing desloratadine The invention relates to a pharmaceutical preparation containing valsartan, which at least comprises active ingredient valsartan or a pharmaceutically acceptable salt thereof and at least two disintegrants in a ratio between 1: 2 and 2;1. The invention also relates to a preparation method of the valsartan preparation, which comprises the following steps of: firstly, pelletizing the valsartan or the pharmaceutically acceptable salt thereof by a rolling method; mixing with at least two disintegrants and other pharmaceutic accessories; and tabletting or filling capsules. Compared with a product prepared by the prior art, the valsartan preparation of the invention has better stability. The method of the invention has simple production process and high production efficiency and is suitable for industrial production.
US20140135340 High Drug Load Tablet The present invention pertains to a high drug load tablet comprising an active ingredient Compound I of formula or a pharmaceutically acceptable salt thereof in an amount from about 30% to 80% in weight of the active moiety based on the total weight of the tablet.
US7772260 Neuroprotectants; reduce side effect of neurotoxic agent; treatment of neuropathies resulting from chemotherapeutic agents used in the treatment of HIV and proliferative disease such as cancer and treatment of inflammatory diseases, neurodegenerative diseases This invention relates to compounds of Formula I and the use of compounds of Formula I as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems. Formula I:
WO2014082581A1 Α-(3,5-dimethoxy benzylidene)-α'-hydrocarbyl methylene cyclic ketone and preparation method thereof Disclosed is an α-(3, 5-dimethoxy benzylidene)-α'-hydrocarbyl methylene cyclic ketone, having a structure as represented by (I) or (II), wherein R is an aryl or alkyl; a preparation method is: mixing cyclic ketone and morpholine, and azeotropically dewatering the mixture to obtain enamine; conducting a condensation reaction between the enamine and 3, 5-dimethoxy benzaldehyde, and condensing with alkyl formaldehyde or aryl formaldehyde under an acidic or alkaline condition to obtain a product. Also disclosed are an α-(3, 5-dimethoxy benzylidene)-α'-hydrocarbyl methylene cyclic ketone or medically acceptable salt thereof, and anti-tumor drug of a pharmaceutically acceptable carrier. By using the above mode and the α-(3, 5-dimethoxy benzylidene)-α'-hydrocarbyl methylene cyclic ketone and preparation method thereof provided by the present invention, the compound splices together and modifies the structures of resveratrol and curcumin (anti-tumor active ingredients in a natural product), so as to obtain an anti-tumor drug having higher activity, thus having good inhibition effect on an epidermal growth factor receptor.
WO2007004621A1 Versipelostatin derivative, anti-cancer agent and processes for production of the derivative and agent [PROBLEMS] To provide a novel anti-cancer agent having a reduced cytotoxicity. [MEANS FOR SOLVING PROBLEMS] A compound represented by the chemical formula 1 or a salt thereof. This compound has an organic group introduced into a given ketone group in VST and, similar to VST, has an effect of inhibiting the induction of GRP78 expression, and therefore can be used as an anti-cancer agent or the like. Further, this compound has a lower toxicity than VST, and therefore can reduce adverse side effects. [Chemical formula 1]
CN102048705A Palonosetron hydrochloride orally disintegrating tablet and preparation method thereof The invention belongs to the field of pharmacy and medical technology, and relates to a palonosetron hydrochloride orally disintegrating tablet and a preparation method thereof. The orally disintegrating tablet comprises the following components in percentage by mass: palonosetron hydrochloride 0.16 to 1.5, mannite 70 to 95, disintegrating agent 1.5 to 15, taste correcting agent 1 to 3, lubricating agent 0.5 to 2, and other auxiliary materials 0 to 15. The manufacturing technology can adopt dry direct tablet compressing. The palonosetron hydrochloride orally disintegrating tablet has the advantages of simple manufacturing technology, low cost and quick effect on indications, is convenient to take, can be disintegrated into fine grains or powder in oral cavity quickly after oral administration, and is particularly suitable for patients who swallow hard and tumor patients with weak physical fitness. The preparation exists in a form of fine grain or powder before reaching the gastrointestinal tract, and the medicine dissolves out in an accelerating manner and is distributed in the gastrointestinal tract in a large area for more absorption points, so that the bioavailability can be improved.
WO2009134511A1 Topical compositions for improving appearance of keratinous surfaces A topical non-dermal filler composition for application to keratinous surfaces comprising at least one injectable dermal filler capable of being absorbed into the epidermal layers of the skin in an amount sufficient to plump the skin and methods for plumping skin by applying the composition of the invention.
EP1483257B1 Quinazoline compounds useful in therapy Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, wherein R1 represents C1-4 alkyl; R2 represents halo, C 1-4 alkyl, C 3-6 cycloalkyl, C3-6 cycloalkyloxy, -SO2(C1-4 alkyl), optionally substituted C1-4 alkyloxy, Het or -OHet; R3 represents a bicyclic group of the formula (II) wherein X and Y are selected from C and N, provided that at least one is C; Ring A together with X and Y represents a 5- or 6-membered aromatic, ring containing 0, l, 2 or 3 nitrogen atoms in the ring; n is ), 1 or 2 L represents a direct link, C1-4 alkylene or C1-4 alkoxyalkylene; R4 represents H, -NR5R6, C3-6 cycloalkyl, -OR7, Het1 or Het4; R5 and R6 are independently selected from H, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-4 alkylene, -SO2(C1-4 alkyl) and optionally substituted C1-4 alkyl. R7 is selected from H, C1-4 alkyl, C1-4 alkoxyalkyl, C3-6cycloalkyl, Het2 and C1-4alkyl-Het3; R8 is H or C1-4 alkyl; Het, Het1, Het2 and Het3 independently represent an optionally substituted 4 to 7 membered saturated heterocyclic group which may be mono- or bi-cyclic and which contains one or more heteroatoms selected from N, O or S; Het4 represents an optionally substituted 5 or 6 membered unsaturated heterocyclic group containing one or more heteroatoms selected from N, O or S; R9is H or C1-4 alkyl; R10 and R11 are independently selected from H and C1-4 alkyl; are useful in the treatment of hypertension, myocardial infarction, male erectile dysfunction (MED), hyperlipidaemia, cardiac arrhythmia, glaucoma and benign prostatic hyperplasia (BPH). They also find utility in the treatment of female sexual arousal dysfunction (FSAD).
CN103435561A Novel D-amino acid oxidase inhibitor and preparation and application thereof The invention provides a novel D- amino acid oxidase inhibitor and a preparation and application thereof. In particular, the invention discloses derivatives of quinoxaline-2,3-diketone, which has a novel structure shown in formula A, as well as a preparation method thereof and an application as an inhibitor of D-amino acid oxidase (DAAO). The compound provided by the invention shows excellent effects of analgesia and blocking morphine analgesia tolerance, and has application value for analgesia, treating opiate drug tolerance, and anti-schizophrenia.
CN103319409A Edaravone compound, medicinal composition thereof, and preparation methods of compound and composition The invention belongs to the technical field of medicines, and concretely relates to an edaravone compound. The structural formula of the edaravone compound is shown in the specification. The X-ray powder diffraction pattern of the edaravone compound measured by using Cu-Kalpha ray is represented by pattern 1. The invention also provides a preparation method of the edaravone compound, a medicinal composition containing the edaravone compound, and a preparation method of the medicinal composition. The dosage forms of the edaravone compound comprise a low capacity injection and a high capacity injection. The edaravone compound has the advantages of large solubility and fast dissolving rate, and the medicinal composition of the edaravone compound has the advantages of good dissolving performance, easy dissolving and compatibility, and high bioavailability.
EP1284771B1 Aerosol container for formulations of salmeterol xinafoate The invention relates inter alia to a container sealed with a valve, which contains a pharmaceutical aerosol formulation comprising (A) particulate salmeterol xinafoate in suspension in (B) a liquefied propellant gas which is 1,1,1,2,3,3,3-heptafluoro-n-propane or 1,1,1,2-tetrafluoroethane and mixtures thereof; said container characterised in that the formulation is substantially anhydrous and remains so over a period of 12 months when stored at 25 °C and at relative humidity of 60 %. Preferably the valve is characterised in that it contains one or more valve seals substantially constructed from a polymer of ethylene propylene diene monomer (EPDM).
CN101422464A Compound fubennikao injection The invention discloses a compound florfenicol injection for curing porcine mycoplasmas infection, which belongs to a medical preparation containing effective components, or an anti-infection animal medicament. Every 100L of injection is prepared by the following materials: 5 to 20kg of florfenicol, 10 to 30L of dimethylformamide, 0.5 to 5kg of doxofylline and the rest is propanediol. The invention adopts a compound preparation of florfenicol and doxofylline, which is highly effective to the mycoplasmal pneumonia of swine, reduces the medicament use times, treats both principal and secondary aspects of diseases and eases the stress response of the body of an affected animal. The injection for curing porcine mycoplasmas infection can be broadly applied to the porcine mycoplasmas diseases, relieve the clinical symptoms caused by the infection of the porcine mycoplasmas and increase the weight of the pig.
CN102579944A Preparation method of medicament (bighead atractylodes rhizome honey paste) for treating infantile diarrhea The invention relates to a preparation method of a medicament (bighead atractylodes rhizome honey paste) for treating infantile diarrhea. The preparation method comprises the following steps of: adding clear water in tuckahoe, common aucklandia root, bighead atractylodes rhizome, fructus amomi, nutgrass galingale rhizome and membrane of chicken gizzard and soaking; placing the components in a pot and boiling to form a paste shape; adding honey and stirring uniformly; and heating to 80 DEG C and stopping fire to form the bighead atractylodes rhizome honey paste. The preparation method is simple; and the bighead atractylodes rhizome honey paste is favorable in taking effect and is especially remarkable in effect for chronic diarrhea caused by persistent dyspepsia.
WO2014160877A1 Prevention and treatment of kidney damage by bile acids A method of treating or preventing kidney injury includes administering to a patient an effective amount of bile acid, a salt thereof, an analog thereof, or a combination thereof. Methods of preventing or retarding, reversing or abolishing the onset of kidney injuries are discussed. This is achieved through the administration of a bile acid, a salt of the bile acid, an analog of the bile acid or any combinations of these compounds. The bile acid abolishes or interferes or down-regulates metabolic pathways leading to the onset of kidney injury. The bile acid also activates metabolic pathways leading to the slowing or reversing or complete abolishment of the progression of acute kidney injury.
WO2014093253A1 Novel aromatic thio compounds as receptor modulators The present invention relates to novel aromatic thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
US20050059654 Method for treatment of depression and anxiety disorders by combination therapy A method is provided of treating depression in mammals, including a human, as well as depression and a concomitant disease, disorder or condition exemplified by, but not limited to, anxiety, sleep disorder and post-traumatic stress disorder. The method comprises administering to the mammal in effective amount a combination of active ingredients comprising a) an alpha-2delta (A2D) ligand or a prodrug thereof, or a pharmaceutically acceptable salt of said A2D ligand or said prodrug and, active agents selected from; (b) a selective serotonin re-uptake inhibitor (SSRI) or a prodrug thereof or a pharmaceutically acceptable salt of said SSRI or said prodrug, (c) a selective noradrenaline re-uptake inhibitor (SNRI) or a prodrug thereof or a pharmaceutically acceptable salt of said SNRI or said prodrug and mixtures of (b) and (c). A pharmaceutical composition comprising a therapeutically effective amount (a) an A2D ligand or a prodrug thereof, or a pharmaceutically acceptable salt of said A2D ligand or said prodrug and active agents selected from; (b) an SSRI or a prodrug thereof or a pharmaceutically acceptable salt of said SSRI or said prodrug, (c) an SNRI or a prodrug thereof or a pharmaceutically acceptable salt of said SNRI or said prodrug and mixtures of (b) and (c) is also provided. Preferred active ingredients for the treatment and the pharmaceutical composition include pregabalin, gabapentin, sertraline and reboxetine.
CN103070824A Ibandronate sodium containing injection The invention relates to an ibandronate sodium containing injection. The injection is prepared by ibandronate sodium and pharmaceutically acceptable auxiliary materials; a pH value of the injection is controlled to be 3.5-4.5 by a phosphate buffer; activated carbon accounting for 0.1% of the total volume of the injection is used for removing a pyrogen; and adsorption of activated carbon to a main medicine is avoided while the pyrogen is removed. An accelerated stability test indicates that the impurity content of the injection is lower than that of the marketed injection, and the quality is stable and controllable.
US7279487 Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors Hydroxynaphthyridinone carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein L, R1a, R1b, R1c, R2a, R2b, R3, R4, and R5 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
WO2008089008A2 Tetrahydrobiopterin prodrugs Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.
US20120264707 Beta-l-2'-deoxy-nucleosides for the treatment of hepatitis b This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.
US20080275010 Compositions and methods to prevent toxicity induced by nonsteroidal antiinflammatory drugs Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.
WO2013059630A1 Methods for treating hcv comprising at least two direct acting antiviral agent, ribavirin but not interferon. The present invention features interferon-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to the subject effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), an inhibitor of cytochrome P450 (e.g., ritonavir), and ribavirin.
WO2014145580A1 Neosaxitoxin combination formulations for prolonged local anesthesia Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin ("NeoSTX") and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX- bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations.
CN1559436A Oral liquid-supplement salt flash-dissloving tablets, and prepn. method therefor An orally-applied flash-dissolving tablet for supplementing salt to human body is prepared from sodium chloride, sodium citrate, potassium chloride, anhydrous glucose, cane sugar, sorbitol, xylitol, tween-80, citric acid and superfine silica gel powder. Its preparing process is also disclosed.
CN103330872A Method for preparing snake wound rehabilitation medicament The invention provides a method for preparing a snake wound rehabilitation medicament. The method comprises the following steps: preparing the following components in parts by weight: 7-10 parts of edible tulip, 10-15 parts of Chinese lobelia, 10-15 parts of angelica root, 15-20 parts of polygonum cuspidatum, 10-15 parts of radix stephaniae tetrandrae, 10-15 parts of rhizoma dioscoreae nipponicae, 10-15 parts of frankincense, 10-15 parts of myrrh, 7-10 parts of mirabilite and the like; soaking the components, except frankincense, myrrh and mirabilite, for 1 hour in water which is 5 times the weight of the medicinal materials,; decocting for 2 hours, and adding frankincense and myrrh to obtain decoction; and filtering, and uniformly mixing with mirabilite. The medicament can be used for remarkably reducing the swelling pain of a wounded limb, accelerating swelling diminishing, pain relieving and toxin eliminating of the wounded limb, promoting rehabilitation and healing of histocyte, effectively preventing and treating of anabrosis, necrosis and amputation complications, preventing and treating sequelae of chronic swelling of the wounded limb, functional disorder and the like caused by snake wound.
CN101357130A Oral microparticles containing pseudoephedrine hydrochloride and cetirizine hydrochloride The invention relates to an oral grain containing pseudoephedrine hydrochloride and cetirizine hydrochloride; the oral grain coats a pseudoephedrine hydrochloride layer which is obtained by coating a coating solution mixed by the pseudoephedrine hydrochloride, a binder, a lubricant and pure water/alcohols is coated at the outside of target core subjects with the grain diameter to be 25 to 40 meshes, and coated by a controlled release film layer outside the pseudoephedrine hydrochloride layer, and a cetirizine hydrochloride layer which is obtained by coating a coating solution mixed by the cetirizine hydrochloride, a binder, a lubricant and pure water/alcohols is coated outside the controlled release film layer; therefore, as the pseudoephedrine hydrochloride and the cetirizine hydrochloride are dispersed in hundreds of grains and the dissolving speed is controlled by the controlled release film layer, the grain obtained has the effects that the absorption is fast, the response of the drug is fast and stable, and the release time of the property of the drug is prolonged.
CN101732241A Cream of butenafine hydrochloride and preparation method thereof The invention belongs to the field of medicine preparations, which in particular relates to butenafine hydrochloride cream and a preparation method thereof. In order to lower the adverse reaction of the traditional butenafine hydrochloride cream and further enhance the curative effect of a medicine, the invention provides the cream containing butenafine hydrochloride and the preparation method thereof. The cream provided by the invention comprises two parts of butenafine hydrochloride liposome and a cream substrate. The preparation method of the cream comprises the following steps: firstly, preparing the butenafine hydrochloride liposome, then preparing the cream substrate, afterwards adding butenafine hydrochloride liposome suspension into the cream substrate according to the preset concentration, stirring evenly and subpackaging so as to obtain the cream.
EP1993572A2 Methods of treating or preventing sinusitis with oxidative reductive potential water solution Provided is a method for preventing or treating sinusitis by administering a therapeutically effective amount of an oxidative reduction potential (ORP) water solution that is stable for at least about twenty-four hours. The ORP water solution administered in accordance with the invention can be combined with one or more suitable carriers. The ORP water solution can be administered alone or, e.g., in combination with one or more additional therapeutic agents.
US20120208832 Process for converting a solid (meth)acrylate copolymer into a dispersed form by means of a dispersing agent The present invention provides a process for converting a solid (meth)acrylate copolymer into a dispersed form by preparing an aqueous dispersion comprising the components (a) a (meth)acrylate copolymer which is composed of free-radical polymerized methyl methacrylate, ethylacrylate and a salt of 2-trimethylammoniumethyl methacrylate, present in solid form as a powder or as a granulate, (b) up to 50% by weight calculated on the (meth)acrylate copolymer (a) of a dispersing agent selected from the groups of (b) i) plasticizers in combination with emulsifiers and/or (b) ii) pharmaceutically acceptable carbohydrates having 6 to 18 carbon atoms with a functional group and (c) water by mixing the components (a), (b) and (c) to give a suspension which becomes an aqueous dispersion during the conversion of the solid (meth)acrylate copolymer into the dispersed form, characterized in that, the (meth)acrylate copolymer is converted into the dispersed form by means of the presence of the dispersing agent at a temperature of less than 50° C.
WO2008126803A1 Ophthalmic composition comprising soluble, cross-linked hyaluronic acid Disclosed is an ophthalmic composition comprising a soluble, cross-linked hyaluronic acid and a pharmaceutically acceptable carrier.
US8642604 Substituted pyrazolo[3,2-d]pyrimidines as anti-cancer agents The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tyrosine kinase, PI3 kinase and mTOR, or PI33 kinase, mTOR and tyrosine kinase.
US20070212368 Proteins The present invention provides methods and compositions for screening, diagnosis and prognosis of breast cancer, for monitoring the effectiveness of breast cancer treatment, and for drug development.
CN101548982A Application of dihydropyridazinone compounds in preparation of pharmaceutical for preventing and treating diabetes The invention relates to an Application of dihydropyridazinone compounds: isookanin or isookanin-7-O-beta-D-glucoside in preparation of pharmaceutical for preventing and treating diabetes. By establishing an alpha-amylase reaction system, the invention performs a in vitro hypoglycemic activity experiment to the isookanin or isookanin-7-O-beta-D-glucoside; the results shows: both of them have substantial hypoglycemic activity, consequently can be used in preparation of pharmaceutical for preventing and treating diabetes. The invention provides a new source for pharmaceutical for preventing and treating diabetes.
US20080160086 Comprising an ingestible matrix within which a calcium source is substantially uniformly and completely dispersed; for preventing bone loss; aid in the uptake and/or metabolism of calcium by the body Oral gel delivery systems for calcium are provided comprising an ingestible matrix within which a calcium source is substantially uniformly and completely dispersed. The delivery systems may optionally include one or more other functional ingredients, for example, functional ingredients that aid in the uptake and/or metabolism of calcium by the body and/or that complement or enhance the function of calcium within the body.
US20080286363 (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one maleate; 3-[(Cyclopentyl-hydroxyphenylacetyl)oxy]-1,1-dimethylpyrrolidinium bromide (glycopyrrolate), and a glucocorticosteroids A medicament comprising, separately or together (A) a compound of formula I in free or salt or solvate form, (B) a glycopyrronium salt; and (C) a compound of formula II for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.
US20110207800 HIV-Dependent expression constructs and uses therefore The invention provides a nucleic acid construct for targeting and killing cells infected with the human immunodeficiency virus (HIV). The construct includes an HIV Tat-dependent promoter operably linked to the coding region for a cell-killing protein, such as anthrolysin-O (anlO), which is partially or fully within an intron defined by a splice donor site and a splice acceptor site. The construct further includes a Rev Responsive Element (RRE). Therapeutic methods of treating HIV infection are also provided.
US8163904 Prepared by reacting free base with an acid in methanol under a nitrogen atmosphere; use in treating a disease which responds to an inhibition of protein kinase activity Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.
CN103690473A Sinomenine preparation and preparation method thereof The invention aims to provide a sinomenine preparation. The preparation is prepared from sinomenine with a proper concentration, ostrich oil, vitamin E with a proper concentration and eucalyptus oil. The preparation method comprises the following steps: heating and melting the ostrich oil into liquid; adding sinomenine powder, and uniformly stirring and dispersing; adding eucalyptus oil and vitamin E, stirring and cooling. According to the preparation, the transdermal effect of sinomenine can be improved and the drug effect of the medicine can be improved; ostrich oil is a pure natural raw material, is capable of reducing skin irritation when used as a drug-loading matrix; in addition, ostrich oil has arthritis resistance and can realize arthritis treatment when used together with sinomenine.
CN1919254A Pharmaceutical compositions and its application The invention provides a pharmaceutical composition comprising total savianolic acid extract and astragalus root total saponin extract, wherein the weight ratio of the two ingredients is 1:9-9:1, the content of total savianolic acid in the extract is lower than 100%, the content of astragalus root saponins is greater than 50%. The invention also provides the use of the pharmaceutical composition in preparing medicaments for treating or preventing acute kidney failure.
EP1738759A1 Inhibition of abnormal cell proliferation with camptothecin and combinations including the same A method for treating diseases associated with abnormal cell proliferation comprises delivering to a patient in need of treatment a compound selected from the group consisting of 20(S)-camptothecin, analog of 20(S)-camptothecin, derivative of 20(S)-camptothecin, prodrug of 20(S)-camptothecin, and pharmaceutically active metabolite of 20(S)-camptothecin, in combination with an effective amount of one or more agents selected from the group consisting of alkylating agent, antibiotic agent, an alkylating agent, antibiotic agent, antimetabolic agent, hormonal agent, plant-derived agent, antigenesis agent and biologic agent. The method can be used to treat benign tumors, malignant or metastatic tumors, leukemia and diseases associated with abnormal angiogenesis.
EP2773348A1 Pharmaceutical composition of omeprazole The present invention refers to oral solid pharmaceutical compositions comprising concentrate omeprazole pellets, processes for the preparation of the same and their use as medicaments, more particularly for the treatment and/or prophylaxis of a gastrointestinal disorder.
WO2009106750A2 Derivatives of 6-heterocyclic-imidazo[l,2-a]pyrroine-2-carboxamides, preparation thereof and therapeutic application thereof The invention relates to compounds of the formula (I) in which: X is an optionally substituted phenyl group; R1 is a hydrogen atom, a halogen, a (C1-C6) alkoxy group, a (C1-C6) alkyl group, a NRaRb group; R2 is an optionally substituted heterocyclic group; R3 is a hydrogen atom, a (C1-C6) alkyl group, a (C1-C6) alkoxy group or a halogen atom; R4 is a hydrogen atom, a (C1-C4) alkyl group, a (C1-C4) alkoxy group or a fluorine atom; said compounds being in the state of a base or an addition salt to an acid. The invention can be used in therapeutics.
US20050075301 Pharmaceutical preparation with RNA as hemostasis cofactor Pharmaceutical preparations which comprise RNA or one or more coagulation-promoting fragments of RNA in amounts sufficient to promote coagulation and to promote fibrinolysis are described. They are in particular advantageously employed together with an activator for hemostatic processes such as factor VII-activating protease (FSAP)
US20080045596 Ep2 Receptor Agonists A compound selected from one of the following: or a salt, solvate, chemically protected form or prodrug thereof, and its use in treating conditions alleviated by agonism of an EP2 receptor.
US20090170839 Aerosol formulation for inhalation containing an anticholinergic agent The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X represents an anion, and containing at least one pharmacologically compatible organic acid and optionally additional pharmacologically compatible adjuvants and/or complexing agents. The cation of formula (1′) is contained in the preparation at a concentration of between 830.22 and 904.2 mg per 100 ml of medicament preparation.
CN103539695A Novel diphenyl ether substituted histone deacetylase inhibitor The invention discloses a diphenyl ether substituted histone deacetylase inhibitor. The diphenyl ether substituted histone deacetylase inhibitor is a compound represented by a formula (I) shown in a drawing, or pharmaceutically-acceptable salts, solvates or chemically protected forms. The compound disclosed by the invention can be applied to the preparation of medicaments for preventing and/or treating diseases related to the out-of-control of histone deacetylase activity and/or the out-of-control of Raf kinase activity.
US20120220644 Use of two microrna moleculars in lung cancer prognosis and medicine preparation The present invention relates to use of two microRNAs in detection of lung cancer prognosis and in medicine preparation. Particularly, the invention relates to a composition comprising two small RNA molecules microRNA-150 and microRNA-886-3p, a device comprising the composition used in detection of lung cancer prognosis and in preparation of medicaments for inhibiting mammal and human lung cancer metastasis. Specifically, the expression levels of microRNA-150 and microRNA-886-3p can be used as the prognostic criteria of lung cancer prognosis, wherein high expression level of the gene combination indicates favorable therapeutic effect. The invention also relates to a device detecting the expression levels of microRNA-150 and microRNA-886-3p in mammalian and human lung cancer and a method for detecting the expression levels of microRNA-150 and microRNA-886-3p in samples.
EP1878433A1 Topical composition comprising magmatites Composition (I) for topical use comprises magmatite-containing rock flour and plant tar. - ACTIVITY : Antipsoriatic; Dermatological; Antiinflammatory; Antiseborrheic. - MECHANISM OF ACTION : None given.
US20110212023 TADG-15: an extracellular serine protease overexpossed in carcinomas The present invention provides DNA encoding a TADG-15 protein as well as a TADG-15 protein. Also provided is a vector capable of expressing the DNA of the present invention adapted for expression in a recombinant cell and regulatory elements necessary for expression of the DNA in the cell. The present invention further provides for methods of inhibiting TADG-15 expression and/or protease activity, methods of detecting TADG-15 mRNA and/or protein and methods of screening for TADG-15 inhibitors. Additionally, the present invention provides for cell-specific targeting via TADG-15 and methods of vaccinating an individual against TADG-15. The methods described are useful in the diagnosis, treatment and prevention of cancer, particularly breast and ovarian cancer.
EP1809312A1 Use of 11-oh-erythravine, erythravine, erytrartine, pharmaceutical compositions and processes for producing these substances The present invention provides the use of molecules for cholinergic and/or serotonergic system models, revealing pharmaceutical compositions comprising 11-OH-erythravine, erythravine, erythrartine, pharmaceutically acceptable isotherals, salts, byproducts and/or solvates thereof, optionally containing other erythrina byproducts, for the treatment of anxiety disorders; processes for obtaining said pharmaceutical compositions are also revealed.
US8598221 Synergistic combination of analgesic compounds The present invention relates to a pharmaceutical composition comprising as active substances: at least one compound of the following general formula (I): and at least one inhibitor of type 2 cyclooxygenase (COX-2), notably for use in the prevention or treatment of pain.
US20070248697 Opthalmic solutions A method of preventing a lowering of concentration of a prostaglandin derivative, the prostaglandin derivative being 16-phenoxy-15-deoxy-15,15-difluoro-17,18,19,20-tetranorprostaglandin F2 α isopropyl ester, the prostaglandin derivative being contained in an ophthalmic solution as an active ingredient. The method including (i) adding to the ophthalmic solution a nonionic surfactant to inhibit the prostaglandin derivative from being adsorbed to a container which contains the ophthalmic solution, the container being made of a resin and (ii) adding to the ophthalmic solution an antioxidant to inhibit decomposition of the prostaglandin derivative.
US20100179091 Treatment of Conditions Related to Shock Techniques are disclosed for prevention or treatment of physiological shock by administering a specific therapeutic agent or combination of therapeutic agents, which is/are able to use smaller volumes of reagent to achieve complete inhibition, than other previously described techniques.
WO2008002246A1 A pharmaceutical composition comprising an ikk2 inhibitor and a second active ingrdient. The present invention provides pharmaceutical compositions comprising an IKK2 inhibitor and a second active ingredient, and their use in therapy.
US20080260858 Universal Procoagulant A thromboplastin reagent comprises: (i) activated sTF, (ii) a metal-chelating lipid, (iii) a metal ion, and (iv) a phospholipid. Activated sTF preferably includes the extracellular domain of TF and an oligohistidine moiety having at least 2 histidine residues, more preferably 2-10 histidine residues. Preferably, the histidine residues are consecutive. Attaching a metal binding domain, such as an oligohistidine tag, to the C-terminus of sTF allows the protein to bind to phospholipid vesicles that contain metal-chelating lipid. Metal complexes of this activated sTF and metal-chelating lipids have all of the desirable expression, handling, and solubility characteristics of sTF, and exhibit procoagulant activities in plasma clotting tests that are comparable to relipidated rTF. In addition, it was discovered that, under some circumstances, Ni-lipids are themselves procoagulant, even in the absence of activated sTF. Further studies indicated that Ni-lipids are potent activators of the contact pathway of blood clotting.
CA2506081C Water-soluble mesoporphyrin compounds and methods of preparation Water soluble tin mesoporphyrin compounds are described. Methods of preparation of water soluble metal mesoporphyrin compounds and pharmaceutical preparations are also described.
EP1542948A2 Novel biphenyl and biphenyl-like cannabinoids Novel biphenyl and biphenyl-like cannabinoid compounds are presented. These compounds, when administered in a therapeutically effective amount to an individual or animal, result in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response useful to treat a number of physiological conditions.
CN101756919A Orally disintegrating tablet containing dimemorfan and preparation method thereof The present invention relates to an orally disintegrating tablet containing dimemorfan and preparation method thereof. The orally disintegrating tablet is quickly absorbed and easily taken (without water) and has high bioavailability, and is suitable for the elderly and children. The orally disintegrating tablet is prepared by taking dimemorfan as raw material and adding proper auxiliary materials according to the technological method described in the present invention. Vitro tests show that the orally disintegrating tablet disintegrates in one minute in 2 ml of water of 37 DEG C (all pass through a No.2 screen).
US20070299040 Composition for Preventing a Cold The present invention relates a composition for preventing cold comprising vitamin C and ginkgetin, a use of the composition for preparing a medicine To prevent cold, a method for preventing cold by using the composition, and method for preparing cold prophylactic. The composition of the present invention has excellent inhibition effect of cold viruses such as influenza viruses, coronaviruses, rhinoviruses an adenoviruses, can remarkably increase immunity, and may be used as health care products for preventing cold or cold medicine without cytotoxicity.
CA2199893C 1,25-dihydroxy-16,22,23-trisdehydro-cholecalciferol derivatives The invention relates to a compound of the formula SEE FORMULA I wherein R is hydroxy and R1 is H2 or CH2, or R is hydrogen or fluoro and RI is CH2. Compounds of formula I are useful as agents for the treatment of hyperproliferative skin diseases, such as psoriasis, neoplastic diseases, such as leukemia, and sebaceous gland diseases, such as acne and sebhorreic dermatitis.
WO2011060179A1 Use of peptide epoxyketones for metastasis suppression The invention provides a method of repressing metastasis of a cancer compromising the administration of a peptide epoxyketone proteasome inhibitor. Furthermore, the method can be performed in combination with the administration of one or more additional therapeutics
WO2008041882A1 Method for affecting viruses by means of an agent based on 2,8-ditioxo-1h-pyrano[2,3-d;6,5-d'] dipyrimidine and 10-aza-analogs thereof (variants) The invention relates to medicine and virology, in particular to a method for affecting viruses by means of an agent based on 2,8-dithioxo-1H- pyrano[2,3-d;6,5-d'] dipyrimidine and 10-aza-analogs thereof. The inventive method consists in using said agent together with an integrase inhibitor, a reverse transcriptase inhibitor or a protease inhibitor in different combinations (variants). The inventive method makes it possible to increase the virus inhibiting efficiency. The invention can be used in medicine and veterinary sciences.
CN103142990A Medicine for treating animal bacterial diseases and preparation method thereof The invention relates to a medicine for treating animal bacterial diseases and a preparation method thereof; each 100mL medicine contains 0.5-2.0g of antimicrobial peptide, 0.2-1.0g of poloxamer 407 and poloxamer 408, wherein the mass ratio of poloxamer 407 and poloxamer 408 is (1:1) to (1:4), 0.3-1.2g of triethanolamine, 1.5-3.5g of glycerol, 1.0-3.0g of tween-80, 0.01-0.03g of butylated hydroxytoluene, 0.01-0.03g of ethylparaben and distilled water. The medicine prepared by the invention is fast and long-lasting in efficiency, is excellent in slow-release effect and easy to control in dosage.
EP2013210A1 Purine derivatives with activity to the adenosine a2a receptor A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein U, R1, R2 and R3 are as defined herein.
US20110130454 Prodrugs of gamma-amino acid, alpha-2-delta ligands, pharmaceutical compositions and uses thereof Prodrugs of alpha-2-delta ligands, pharmaceutical compositions of prodrugs of alpha-2-delta ligands, methods of making prodrugs of alpha-2-delta ligands, and methods of using prodrugs of alpha-2-delta ligands and pharmaceutical compositions of prodrugs of alpha-2-delta ligands to treat various diseases are disclosed.
US7572826 Thiophene-carboxamide derivatives and their use as inhibitors of the enzyme IKK-2 The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
CN101851196B 2-(1H) quinolinone derivative, medical composition, preparation method and application thereof The invention relates to a 2-(1H) quinolinone derivative 1-11, a preparation method thereof, a medicament composition containing the 2-(1H) quinolinone derivative 1-11 and used for treating hepatitis B and application of the derivative and the medicament composition thereof in preparing an anti-hepatitis B inhibitor medicament and an anti-hepatitis B medicament.
US20090082301 Gene therapy for renal failure The present invention relates to recombinant vectors expressing the BMP-7 polypeptide in host cells and to pharmaceutical compositions comprising such recombinant vectors. The invention also encompasses methods for prevention and/or treatment of both acute and chronic renal failure in mammals, advantageously in dogs and cats, by administration of the recombinant vectors and pharmaceutical compositions of the invention.
CN102000231A Medicine composition for treating osteopathic diseases The invention relates to a medicine composition for treating osteopathic diseases, which is prepared from the following substances in parts by weight: 20 to 50 parts of rhubarb, 20 to 50 parts of safflower, 20 to 50 parts of grass-leaved sweetflag, 10 to 30 parts of henbane, 10 to 30 parts of rhododendron molle, 10 to 30 parts of lanceolate jasmine root, 20 to 50 parts of sambucus thunbergiana, 10 to 30 parts of hemlock parsley, 20 to 50 parts of mahonia, 20 to 50 parts of narrowleaf rockvine root herb, 10 to 30 parts of native copper, 10 to 30 parts of rhizoma drynariae, 10 to 30 parts of teasel root, 10 to 30 parts of tuber pinellia, 10 to 30 parts of arisaema cum bile, 20 to 50 parts of periplocae, 20 to 50 parts of achyranthes and 10 to 30 parts of fibraurea recisa. The medicine does not have toxic or side effect, is convenient to use and has short cure time, the diseases can not easily recur after being cured, and the medicine can be effectively used for treating the osteopathic diseases.
US20110195920 Biodefenses using triazole-containing macrolides Use of macrolide and ketolide antibiotics for the treatment of acute exposure and diseases caused by biodefense pathogens is described.
US7579362 3-(6-p-Tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane; treatment of psychotic disorders such as schizophrenia, mania, depression and anxiety; neurodegenerataive disorders such as senile dementia, Alzhelmer's disease and other intellectual impairment disorders The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
CN102125582A Silicon lattice active crystals The invention provides a medicament, i.e., silicon lattice active crystals, for treating hypertension and diabetes. The silicon lattice active crystals consist of the following components in percentage by weight: 20 percent of sodium tetraborate, 8 percent of magnesium oxide, 9 percent of potassium carbonate, 7 percent of zinc oxide, 10 percent of strontium carbonate and 6 percent of dichromium trichloride and are prepared by the following steps of: heating in a quartz crucible to 1,300 DEG C and smelting for 24 hours; and injecting into a granulating machine to prepare silicon lattices with diameters between 3mm and 10mm. When the silicon lattice active crystals are used, 30g of silicon lattices are soaked into water with temperature between 80 DEG C and 100 DEG C for 30 minutes, so that inorganic elements including trivalent chromium Cr<3+>, magnesium Mg, zinc Zn, potassium K, strontium Sr, boron B and silicon Si are released; and the soaking water has an extremely good effect for treating hypertensive and diabetic patients when being drunk.
WO2008053495A1 A novel crystalline form of atorvastatin sodium A novel crystalline form of atorvastatin sodium. The said crystalline atorvastatin sodium has characteristic X-ray powder diffraction pattern and is highly pure with purity above 99.5%.
CN101029037A 2-benzo(C) foroxone compound, its production and use A 2-benzo[c] furanketon compound used for preparing the medicines to treat cerebral ischemia and convulsion is prepared through nitrifying, reducing and diazotizing reactions. It has high activity and liposolubility.
WO2010072754A1 HYDROSOLUBLE [6)O-α-D-GLCP-(1→]n-6-O-β-D-GLCP-(1→-PHENOLIC DERIVATIVES WITH DERMOCOSMETIC, NUTRITIONAL AND THERAPEUTIC APPLICATIONS, AND COMPOSITIONS CONTAINING SAID WATER SOLUBLE COMPOUNDS The invention relates to [6)-O-α-D-Glcp→]1 →]n-6-O-β-D-Glcp-(1→-phenolic derivatives. These [6)-O-α-D-Glcp-(1→]n-6-O-β-D-Glcp-(1→-phenolic derivatives of selected phenolics are new, have a solubility in water higher than that of their parent O-β-D-Glcp- (1→-phenolic derivatives and have useful applications in cosmetic, nutrition and pharmaceutical compositions, such as treating or preventing oxidative stress, a cancer, a cardiovascular disease, a bacterial infection, a viral infection, a fungal infection, a UV- induced erythema, an allergy, a metabolism disorder, diabetes, an obesity, an hormonal disorder, a bone disease, a pain, a brain disease, a mouth or teeth disease, an inflammatory or immune disorder.
EP2506712A1 Morphinan derivatives for the treatment of drug overdose The instant application relates to morphinan derivatives of Formula I with sustained effectiveness in treating drug toxicity and overdose:
EP1383752B1 Deuterated 3-piperidinopropiophenone and medicaments containing said compounds The invention relates to deuterated 3-piperidinopropiophenone and their physiologically acceptable salts. The invention also relates to the use of deuterated 3-piperidinopropiophenone in the treatment of muscular diseases and in the production of medicaments for the treatment of muscular diseases. The invention further relates to pharmaceutical compositions containing deuterated 3-piperidinopropiophenone and their physiologically acceptable salts for the treatment of muscular diseases, in addition to their pharmaceutically acceptable adjuvants and/or additives.
US8193249 Triptolide analogs for the treatment of autoimmune and inflammatory disorders The present invention provides synthetic methods and compositions for treatment of autoimmune and anti-inflammatory disorders comprising administering an effective amount of a derivative of triptolide alone or in combination or alternation with other anti-autoimmune or anti-inflammatory compounds.
US7390873 Microbiocides; bactericides A novel class of cationic peptides having antimicrobial activity is disclosed. These peptides can be encompassed by the formulas: X1X1PX2X3X2P(X2X2P)nX2X3(X5)0; (SEQ ID NO:23) X1X1PX2X3X4(X5)rPX2X3X3; (SEQ ID NO:24) X1X1X3(PW)uX3X2X5X2X2X5X2(X5)0; and (SEQ ID NO:25) X1X1X3X3X2P(X2X2P)nX2(X5)m; (SEQ ID NO:26) wherein: m is 1 to 5; n is 1 or 2; o is 2 to 5; r is 0 to 8; u is 0 or 1; X1 is Isoleucine, Leucine, Valine, Phenylalanine, Tyrosine, Tryptophan or Methionine; X2 represents Tryptophan or Phenylalanine X3 represents Arginine or Lysine; X4 represents Tryptophan or Lysine; and X5 represents Phenylalanine, Tryptophan, Arginine, Lysine, or Proline. The invention also provides a method of producing a cationic peptide variant having antimicrobial activity.
US20090005371 Substituted Fused [1,2]Imidazo[4,5-C] Ring Compounds and Methods Fused [1,2]imidazo[4,5-c] ring compounds, e.g., fused [1,2]imidazo[4,5-c]quinolines and [1,2]imidazo[4,5-c]naphthyridines, with a substituent, e.g., a substituted alkoxy substituent, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
US20130004601 Appetite regulating dietary supplement A dietary supplement for regulating the appetite of an individual is described. The dietary supplement comprises at least one mechanical satiety regulator, and at least one chemical satiety inducer, and may additionally comprise at least one thermogen, and/or at least one side effect remover. The dietary supplement induces satiety based on a combination of occupying part of the volume of the stomach, inducing sending signals to the brain in respect of satiety. Furthermore the dietary supplement may maintain or increase metabolism and reduce side effects such as the amount of produced flatulence. The dietary supplement may comprise fibre, whey, plant parts from plants e.g. of the genus Capsicum and plant parts from a species e.g. of the genus Mentha.
WO2007131357A1 Pharmaceutical composition having reduced abuse potential A pharmaceutical paste composition comprising an active ingredient such as an addictive substance, a controlled release agent, and a pharmaceutically suitable aqueous or non-aqueous carrier. The composition may comprise one or more of a clay, or an oily, waxy, or fatty substance. The composition may be filled into a capsule or other dispensing device. The composition may reduce dose dumping of an active ingredient. Methods of making and using the composition are also described.
CN103467383A Conjugate of paeonol and ozagrel, pharmaceutical composition and medical application of conjugate The invention discloses a conjugate of paeonol and ozagrel, a pharmaceutical composition and medical application of the conjugate. The conjugate of paeonol and ozagrel has a structural formula shown in the specification. The invention also discloses application of the conjugate of paeonol and ozagrel in preparation of a medicine for preventing or treating cardiovascular and cerebrovascular diseases caused by platelet aggregation, and also discloses the pharmaceutical composition of the conjugate of paeonol and ozagrel, and a carrier containing the conjugate of paeonol and ozagrel or a pharmaceutically acceptable vector. The compound has the effect of preventing or treating cardiovascular and cerebrovascular diseases caused by platelet aggregation, and especially treating the thrombotic cardiovascular and cerebrovascular ischemia or infarct and other diseases.
US6996473 Method for screening and producing compound libraries A secondary compound library produced by a method of screening a compound library or portion thereof by absorption is provided. The method includes a step (i) that screens a primary compound library or portion thereof having a plurality of test samples containing isolated compounds or isolated mixtures of compounds per test sample by generating an in vivo absorption profile for each of the test samples from initial dose data and from in vitro bioavailability data comprising permeability and solubility data for each of the test samples, wherein the absorption profile includes at least one of rate of absorption, extent of absorption, and concentration of a test sample. Step (ii) produces a secondary compound library that includes at least one compound from the primary compound library having a desired absorption profile.
WO2012173226A1 Pharmaceutical preparation containing polystyrenesulfonic acid salt [Problem] To provide a pharmaceutical preparation containing a polystyrenesulfonic acid salt, which has a reduced sensation of water absorption and a reduced sensation of burning upon ingestion compared with conventional products and contains an excipient in a reduced amount. [Solution] A pharmaceutical preparation containing a polystyrenesulfonic acid salt as an active ingredient, which comprises core granules each comprising the polystyrenesulfonic acid salt and a binder, wherein each of the core granules has at least one coating layer formed on the surface thereof, and wherein the coating layer comprises at least (a) a water-soluble polymer or a water-insoluble polymer and (b) a sugar or a sugar alcohol.
US20090074890 Substituted Triazoles as Sodium Channel Blockers Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier (I), (II), (III).
US20080026052 Oral Dosage Forms with Therapeutically Active Agents In Controlled Release Cores and Immediate Release Gelatin Capsule Coats The present invention relates to oral dosage form with active agents in controlled release cores and in immediate release gelatin capsule coats.
CN101972232A Eudragit S100 coated curcumin pectin microsphere and preparation method thereof The invention discloses an eudragit S100 coated curcumin pectin microsphere. The microsphere is prepared by the following steps: preparing the curcumin pectin microsphere, and coating, wherein the curcumin pectin microsphere is prepared from curcumin and pectin, the mass ratio of the curcumin to the pectin is 1:(1-6), the grain size of the pectin microsphere is between 50 and 80 mu m, the loading rate is between 10 and 31 percent, and the entrapment rate is between 40 and 60 percent; and the coating material is Eudragit S100, the mass ratio of the Eudragit S100 to the curcumin pectin microsphere is (5-10):1, the grain diameter of the coated microsphere is between 150 and 210mu m, and the loading rate is between 0.8 and 1.5 percent. The colon targeting pectin coated microsphere prepared from the curcumin can specifically release the curcumin under a colon physiological condition, the medicament is concentrated in the colon region, and the local medicament concentration is improved, so the function of effectively treating colon cancer can be achieved.
CN102210647A Gel sustained-release preparation capable of improving ring-close rates of camptothecin and derivative lactone ring thereof The invention belongs to the technical field of medicine and in particular relates to a gel sustained-release preparation capable of improving ring-close rates of a camptothecin and a derivative lactone ring thereof. The gel sustained-release preparation is composed of a amphipathy block copolymer, an anti-tumor medicine in effective dose and a solvent, wherein the amphipathy block copolymer is constructed by taking a polyethylene glycol as a hydrophilic block and a polyester as a lyophobic block, and the tail end of the block polymer is connected with a functional end group; the anti-tumor medicine is selected from the camptothecin and the derivative thereof. The gel preparation can be used for effectively improving the ring-close rates of the born camptothecin and derivative lactone ring thereof. The preparation can be administrated through injection; and the encapsulated medicine can be slowly released after the preparation is gelled in situ in a body. The thermo-sensitive hydrogel preparation can be used for enhancing the activity of the medicine, and obviously reducing the required medicine dosage, and can be injected into a tumor or around the tumor, or administrated in a tumor cavity after the surgery; and the gel sustained-release preparation has a passive targeting function, can be used for effectively reducing the general reaction of the medicine and can be used for treating the tumor at different stages.
EP2394651A1 Penciclovir or Famciclovir for the Treatment of Recurrent Genital Herpes With a One-Day Application A method for the treatment of recurrent genital herpes, in mammals, including humans, which method comprises administering to the mammals in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a treatment period of one day.
WO2009017625A1 Treatment of depression, phychosis, and anxiety The use of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) for treating affective disorders, such as depression, psychosis, or anxiety, is described.
CN101829103B Application of flavonoid quercetin dimmer as medicament for treating viral hepatitis B The invention relates to the application of flavonoid quercetin dimmer as the medicament for treating viral hepatitis B, in particular to the application of flavonoid quercetin dimmer or pharmaceutically acceptable salt thereof to the preparation of the medicament for eliminating HBsAg and HBeAg and inhibiting HBV DNA replication. The flavonoid quercetin dimmer or pharmaceutically acceptable salt thereof has obvious HBsAg and HBeAg inhibiting activity, and at the concentration of 100mcg/ml, the flavonoid quercetin dimmer pharmaceutically acceptable salt thereof has the HBsAg eliminating strength of 65.7% and the HBeAg eliminating strength of 44.8% which are respectively 4.1 times and 2.7 times higher than the positive control medicament of Alpha-interferon and has the HBV DNA inhibiting ratio of 44.8% which is 117% of the HBV DNA inhibiting ratio of the Alpha-interferon at the highest test concentration. Therefore, the flavonoid quercetin dimmer or pharmaceutically acceptable salt thereof can be expectedly used for preparing the non-nucleoside medicament for eliminating HBsAg and HBeAg, inhibiting HBV DNA replication and treating viral hepatitis B.
EP2046316A1 Antiviral use of cationic surfactant Cationic surfactants derived from the condensation of fatty acids and esterified dibasic amino acids, such as from lauric acid and arginine, in particular the ethyl ester of the lauramide of the arginine monohydrochloride (LAE), may be used for the protection against the growth of the microorganisms. The cationic surfactants of this type are also effective against virus infections. Addition of LAE to cultures of Herpes virus type 1 Vaccinia virus and bovine parainfluenzae 3 virus leads to nearly complete reduction of the virus organisms in these cultures, such effects being observed after 5 and 60 minutes.
WO2008147243A1 Binuclear nirtosyl-iron complexes with benzo-trans-heterocyclic derivatives and a method for the production thereof The invention relates to binuclear nirtosyl-iron complexes with benzo-trans-heterocyclic derivatives of general formula [Fe2(SR)2(NO)4], wherein R is of (I), in which x is NH, S or O and R1 is lower alkyl, to a method for production thereof, to the use thereof in the form of an antitumoral medicinal agent, to a nitrogen monoxide donor based thereon, to a pharmaceutical composition containing said complexes in an effective quantity and to a set used for treating oncological diseases.
WO2008047633A1 Aliphatic compound-containing skin whitening agent Disclosed is a skin whitening agent having excellent skin whitening effect, while having high safety to the human body and high melanin production inhibiting effect. Specifically disclosed is a skin whitening agent characterized by containing an aliphatic compound represented by the formula I below, a stereoisomer thereof, an optical isomer thereof, or a pharmaceutically acceptable salt of any of them. [chemical formula 1] I (In the formula, R represents a hydrogen or a C1-10 linear or branched alkyl group; and R' represents a hydrogen or a C1-10 linear or branched alkyl group, or alternatively OR' is combined to form a carbonyl group.)
CN101812066A Pyrazolo N-substituted dehydronorcantharidin imide derivative as well as synthesis method, activity test method and application thereof The invention discloses a pyrazolo N-substituted dehydronorcantharidin imide derivative as well as a synthesis method, an activity test method and application thereof, belonging to the field of cantharidin derivatives. The pyrazolo N-substituted dehydronorcantharidin imide derivative has a structural general formula shown as a formula 1: in the formula 1, R1 is H, C1, F, CH3, OCH3, OH or NO2; and R2 is 2-phenyl-2H-1,2,3-triazole-4-substituent or quinoxaline-2-substituent. The novel N-substituted dehydronorcantharidin imide derivative introduces five-membered heterocyclic pyrazole rings into norcantharidin substituted arylamine and has favorable anti-tumor activity.
WO2007060802A1 Solid pharmaceutical preparation and pharmaceutical preparation composition It is intended to provide a solid pharmaceutical preparation and a pharmaceutical preparation composition containing a stable pranlukast hydrate which elutes quickly and in which the elution rate thereof is not likely to change even if it is stored in an unpacked condition. A granulated substance contains 0.02 to 0.15 part by weight of low-substituted hydroxypropylcellulose and 0.1 to 0.6 part by weight of one or more excipients selected from lactose, white soft sugar and mannitol relative to 1 part by weight of the pranlukast hydrate, elutes quickly, shows a stable elutability and has a small change in the elution rate with time.
US20080299168 Stabilized Polymeric Delivery System The invention relates to a delivery system for the sustained and controlled delivery of a group of bioactive agents. More particularly, the invention relates to a delivery system and a method for delivery of a bioactive agent containing a nucleophilic functional group by means of a biodegradable, sustained-release implant. The implant may be a preformed implant, microparticles or an in situ formed implant. The implant includes a biodegradable thermoplastic polymer, the bioactive agent having a nucleophilic group substituent and a stabilizing associate as well as other optional components. The combination of the stabilizing associate with the bioactive agent prevents and/or minimizes and/or lessens degradation of the thermoplastic polymer by the bioactive agent.
CA2184375C Oligonucleotide n3'-p5' phosphoramidates: synthesis and compounds; hybridization and nuclease resistance properties Modified oligonucleotides 3'-NHP(O)(O-)O-5' phosphoramidates were synthesized on a solid phase support. The phosphoramidate analogs were found to have significantly increased resistance toward phosphodiesterase digestion. Thermal dissociation experiments demonstrated that these compounds form more stable duplexes than phosphodiesters with complementary DNA and particularly RNA strands. Further, the phosphoramidate analogs can also form stable triplexes with double-stranded DNA target, where under similar conditions parent phosphodiester compounds failed to do so.
CN103739733A Anti-duck virus hepatitis (DVH) subprostrate sophora polysaccharide and molecular modifier thereof The invention relates to anti-duck virus hepatitis (DVH) subprostrate sophora polysaccharide and a molecular modifier thereof, belonging to the technical field of preparation of Chinese veterinary medicaments. Different alcohol precipitation fractions of the subprostrate sophora polysaccharide are extracted. An anti-duck virus hepatitis (DVH) active site is screened by means of repeated clinical tests. The following optimal conditions for modifying a subprostrate sophora polysaccharide active site by means of chlorosulfonic acid-pyridine sulfation are determined by using an orthogonal method: the reaction temperature is 95 DEG C, the reaction time is 2 hours, and the ratio of chlorosulfonic acid to pyridine is 1:5. According to infrared spectroscopic analysis, an obtained product is subprostrate sophora polysaccharide sulfate, the saccharide content is up to 83.77 percent, the sulfate content is up to 39.33 percent, and the yield is up to 117.33 percent. The subprostrate sophora polysaccharide sulfate is remarkably superior to the subprostrate sophora polysaccharide in resistance of DHV-1 infection of duck fetal liver cells and curative effect on DVH. The obtained anti-DVH subprostrate sophora polysaccharide active site sulfate is high in saccharide and phosphate contents and yield, and has a good curative effect on DVH.
US20100130444 Complexes of prostaglandin derivatives and monosubstituted, charged beta-cyclodextrins The present invention relates to water-soluble, non-covalent complexes of a group of prostaglandin derivatives including latanoprost and monosubstituted, charged β-cyclodextrins, as well as uses of these complexes in therapeutic compositions that are administered topically for treating intraocular hypertension and glaucoma.
US20090312303 Antidiabetic Bicyclic Compounds Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
CN101675932A Composition for preventing and treating amyotrophic lateral sclerosis The invention relates to a composition for preventing and treating amyotrophic lateral sclerosis. The invention discloses a use of homocysteine downregulator in the preparation of a composition for preventing, alleviating or treating the amyotrophic lateral sclerosis of mammal, wherein the downregulator is a folic acid or a mixture of the folic acid and a vitamin B12. The downregulator can effectively alleviate the amyotrophic lateral sclerosis of mammal, reduce the level of inflammatory factors in the spinal cord of mammal, reduce the level of apoptosis protein in the spinal cord, and improvethe level of anti-apoptotic protein in the spinal cord.
CN103520095A Gastrodin injection and preparation process thereof The invention provides a gastrodin injection and a preparation process thereof, and the gastrodin injection can be used for reducing white spots and white blocks occurring during storage, improving the clarity, guaranteeing the safety of medication and meanwhile guaranteeing better stability. According to the gastrodin injection and the preparation process thereof, lactose, procaine hydrochloride, sodium hyposulfite, niacinamide and glycine are used as auxiliary materials; the white spots and the white blocks occurring during storage can be reduced, the clarity can be improved and the safety of medication can be guaranteed after proportioning; but meanwhile, we found that the gastrodine content is obviously reduced after the gastrodin injection is stored for a period of time after the auxiliary materials are added; after the addition sequence of the auxiliary material is adjusted by using the special technology, the content of the gastrodine in the gastrodin injection is still stable after long-time storage, so that the validity of the clinical medication is guaranteed.
EP1875900A2 JAK/STAT pathway inhibitors and the use thereof for the treatment of osteoarthritis The role of JAK/STAT signal transduction pathway cellular mechanisms that lead to the onset and progression of degenerative joint diseases or disorders such as osteoarthritis (OA) is disclosed. Certain known effective OA therapeutics such as hymenialdisine, debromohymenialdisine, and its variants and derivatives are shown to function as JAK3-specific inhibitors, which downregulate steady state mRNA levels of key cellular components involved in cartilage degradation. Another JAK3-specific inhibitor, not previously known as an OA therapeutic, is shown to downregulate steady state mRNA levels of various cellular components involved in cartilage degradation in a manner identical to that of the known OA therapeutics.
CN103285394A Use of nitrated lipids for treatment of lipid disorders and obesity, and lipid- and obesity-related conditions The present invention relates to methods of treating lipid disorders, lipid-related disorders or conditions, obesity and obesity-related disorders using nitrated lipids. In particular, the methods comprise administering effective amounts of nitrated fatty acids or esters thereof in order to reduce one or more of triglycerides, free fatty acids, body weight, cholesterol, urine protein excretion and oxidative stress or increase the level of plasma HDL in a subject.
CA2348380C Aromatic derivatives and iron complexes thereof for the use as normalising agents of the iron level The present invention is directed to aromatic derivatives of formula (I), wherein: R1 is (a), wherein R3 and R4 are selected from between H and OH, provided that R3 and R4 are not simultaneously H, and R2 is H; or R1 and R2 taken together, are (b), wherein R5 is selected from between CH3 and (CH2)5OH, to the iron complexes thereof, and to their use for the preparation of pharmaceutical compositions for the normalisation of iron level.
WO2012157290A1 Prophylactic/ameliorating agent for non-alcoholic steatohepatitis [Problem] The present invention provides a medicinal agent for treating/preventing non-alcoholic steatohepatitis, which can be ingested easily, is derived from a natural material, has no adverse side effect, and is safe. [Solution] For preventing/ameliorating non-alcoholic steatohepatitis or hepatic fibrosis, astaxanthin or an ester thereof is administered.
CN102366404A Propofol medium-long-chain fatty emulsion The invention discloses a propofol medium-long-chain fatty emulsion, which is made from the following components of: by weight, 10-20 parts of propofol, 50-100 parts of soybean oil, 50-100 parts of medium-chain triglyceride, 20-25 parts of glycerin, 6-12 parts of phosphatidylcholine bilayer, 0.02-0.05 part of sodium hydroxide, 0.3-0.6 part of oleic acid and injection water.
US20100105682 Cyclopropyl-piperazine compounds as calcium channel blockers Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of compounds containing both a piperazine ring and a cyclopropyl ring are disclosed of the general formula (I) where X1 and X2 are linkers.
CN1857201A Slow released anticancer injection with both blood vessel inhibitor and its synergist The slow released anticancer injection with both blood vessel inhibitor and its synergist consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The effective anticancer component is blood vessel inhibitor and/or blood vessel inhibitor synergist selected from hormone anticarcinogen and/or platinum compound. The slow releasing supplementary material is one of difatty acid-sebacic acid copolymer, poly (erucic acid dipolymer-sebacic acid), poly (fumaric acid-sebacic acid), polylactic acid, etc or their composition. The suspending agent is carboxymethyl cellulose, etc. and has viscosity of 80-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for use alone or together with chemotherapeutic and/or radiotherapeutic medicine.
CN103340832A Pantoprazole sodium freeze-dried powder injection for injection and preparation method thereof The invention discloses a pantoprazole sodium freeze-dried powder injection for injection. Additive contained in the freeze-dried powder injection comprises tromethamine; and the preparation method comprises the following steps: preparing a medicinal liquid, and performing freeze-drying. The freeze-dried powder disclosed by the invention is high in stability, less in variety of auxiliary materials and safer in preparation; and meanwhile, the process is simple and meets the requirements for mass production.
WO2013061004A8 Novel disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated diseases The present invention relates to novel disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds corresponding to the following general formula (I): , to the pharmaceutical compositions containing these compounds and also to the use of these compounds and of these compositions for the treatment of chemokine-mediated diseases.
US20090118200 Proline bis-amide orexin receptor antagonists The present invention is directed to proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
US20130259904 Prasugrel containing quickly released stable oral pharmaceutical compositions Prasugrel containing quickly released stable oral pharmaceutical compositions containing micronized prasugrel base, and starch or a starch derivative, and processes for the preparation thereof, and the use thereof for treating atherothrombotic events of patients suffering from acute coronary syndrome in which patients were subjected to percutaneous coronary intervention.
WO2011159717A1 Inhibition of pro-inflammatory cytokine induced response Method and compositions for reducing the inflammation after cytokine exposure of an islet cell transplant without affecting the viability and potency are disclosed herein. The present invention describes a composition comprising Withaferin A (WA), a steroidal lactone derived from Withania somnifera to effectively block NF-kB activation in beta cells, minimize cytokine-induced cell death and improve survival of transplanted islets. The method of the present invention involves identifying a subject having islet cells in need of treatment; and providing a effective amount of a Withaferin A composition disposed in a pharmaceutically acceptable carrier in an amount sufficient to reduce the inflammation after cytokine exposure without affecting the viability and potency of the islet cell population.
WO2004085448A3 Unsaturated phosphinyl-phosphonate phosphate transport inhibitors A method of inhibiting phosphate transport in a subject in need of phosphate transport inhibition includes the step of administering to the subject an effective amount of a compound containing a double bond or triple bond directly adjacent to a phosphinyl phosphonate group. The invention also includes compounds containing such unsaturated phosphinyl phosphonate groups and methods of preparing these compounds.
CN102337297A Mbr-FPGS (folylpolyglutamate synthetase) efficient expression vector and construction method and application thereof The invention discloses an mbr-FPGS (folylpolyglutamate synthetase) efficient expression vector. In the vector, a plasmid vector is pEGFP-C1, an mbr sequence with the length of 279bp is contained on the upstream of a cytomegalovirus (CMV) promoter of the pEGFP-C1, and a protein coding region of FPGS is contained between two restriction enzyme cutting sites, namely Hind III and EcoR I of the pEGFP-C1; and the mbr sequence is shown in a sequence table 2. An IC50 result of the constructed mbr-FPGS efficient expression plasmid which is measured by a Western Blot experiment and a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) experiment proves that: the FPGS expression level of the mbr-FPGS efficient expression plasmid is improved by 30 percent (p is less than 0.05) compared with that of an FPGS comparison plasmid, the mbr-FPGS efficient expression plasmid can obviously improve the sensitivity of cancer cells to methotrexate (MTX) and has a certain dose-time dependence,and the IC50 value (72h) of an mbr-FPGS efficient expression group cell is 2.63ng/ml which is one seventh (p is less than 0.05) of the IC50 value (19.01ng/ml) of a comparison group cell approximately.
WO2012064130A3 Colon-targeted celecoxib precursor compound and pharmaceutical composition containing the compound as an active ingredient for treating or preventing colonic diseases The present invention relates to a celecoxib precursor compound and to a pharmaceutical composition containing the compound as an active ingredient for treating or preventing colonic diseases. More particularly, the present invention relates to a celecoxib precursor compound and to a pharmaceutical composition containing the compound as an active ingredient for treating or preventing colonic diseases, wherein the celecoxib precursor compound is not absorbed and stays in a stable state in a stomach and small intestine but metabolized in the colon by means of an enzyme so as to exhibit medicinal effects, thus enabling the utilization of celecoxib, which is a COX-2 inhibitor, in treating or preventing colonic diseases.
US20090253807 Aqueous suspension preparations Addition of polyvinylpyrrolidone and a water-soluble anionic macromolecular compound to an aqueous suspension of a hardly soluble drug allows to provide an aqueous suspension in which aggregation of drug particles, formation of macro crystals from suspended particles and formation of secondary particles from deposited particles are prevented, and adhesion and adsorption to containers made of plastics, e.g., polypropylene or polyethylene, are avoided. As it has a good redispersibility, the aqueous suspension is useful as eye drops, nasal drops, ear drops, injections, oral preparations, liniments and lotions.
US7098364 2-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert-butylaminoethanol hydrochloride; treating asthma and bronchitis The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 is H, chlorine, or bromine; R2 is electron attractive groups selected from the group consisting of CF3, CN, fluorine, CH3SO3, CF3SO3, and NO2; R3 is linear or branched alkyl having 1 to 10 carbon atoms, linear or branched alkoxyalkyl having 2 to 10 carbon atoms, aliphatic alcohol having 1 to 10 carbon atoms, or cycloalkyl having 3 to 6 carbon atoms. The invention also relates to methods for preparing the said compounds and the composition comprising the same. The compounds of the present invention have the effect of β2-receptor agonist and can be used for the treatment of asthma and bronchitis
CN1623544A Preparation of injection amoxicillin subaton A powder injection of amoxicillin-sulbactam is prepared from amoxicillin and sulbactam (or sulbactam sodium) proportionally. Its advantages are low dosage, high curative effect, and less by-effect.
US20080318884 Methods for Altering Gene Expression and Methods of Treatment Utilizing Same The present disclosure describes methods for altering the expression of a target gene comprising a rare cluster of codons, including, but not limited to, trinucleotide repeats. The method utilizes, in part, on amino acid deprivation or the limiting of specific charged tRNAs. The methods for altering target gene expression may be used in treatment methods to treat diseases in a subject organism in need of such treatment. Such methods for altering target gene expression have not been heretofore recognized in the art. Exemplary diseases that may be treated using the methods of the present disclosure include any disease where altering the expression of the target gene would provide treatment. Such diseases include all forms of cancer, ageing, infectious disease, metabolic disorders, inflammation, neurological disorders, diabetes, psychiatric disorders and diseases associated with trinucleotide repeats.
US20080152616 Amphiphilic block copolymer and polymeric compostition comprising the same for drug delivery The present invention relates to an amphiphilic block copolymer of a hydrophilic block and a hydrophobic block with a terminal hydroxyl group wherein the terminal hydroxyl group of the hydrophobic bock is substituted with a tocopherol or cholesterol group. It also relates to polymeric compositions capable of forming stable micelles in an aqueous solution, comprising the amphiphilic block copolymer and a polylactic acid derivative wherein one or more ends of the polylactic acid are covalently bound to at least one carboxyl group.
US20080299184 diagnosing nonsmall cell lung cancer by analyzing PCDH20 gene in a lung sample; measurement of the expression level of the cancer-suppressing gene and methylation of genomic DNA It is an object of the present invention to provide a cancer-suppressing agent comprising a novel cancer-suppressing gene based on the discovery of such cancer-suppressing gene. The present invention provides A cancer-suppressing agent which comprises PCDH20 gene or a homologous gene thereof.
WO2011080982A1 Oil or fat composition for prevention or treatment of depression or depressed conditions Disclosed is an oil or fat composition characterized by containing a medium-chain fatty acid having 8 to 10 carbon atoms and a long-chain fatty acid having 12 to 24 carbon atoms both in the forms of triglycerides, wherein the content ratio of the long-chain fatty acid in the total amount of the medium-chain fatty acid and the long-chain fatty acid is 25 to 90 mass%. The composition is effective for the prevention or treatment of depression or depressed conditions, is highly safe, and causes no adverse side effect when ingested continuously.
US20080293677 Use of Alternating Amine and Non-Amine Bisphosphonate Combinations For Treating Osteoporosis A method of treating osteoporosis in a human in need thereof by administering alternating amine and non-amine bisphosphonates in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit in the treatment of osteoporosis. Particularly, the method involves administration of a time-dependent dose of more than one bisphosphonate, specifically, alternating administration of a first bisphosphonate with a second bisphosphonate, wherein at least one bisphosphonate is administered in a stepped-up dosage amount.
EP0946177B1 METHOD OF INHIBITING BIOSYNTHESIS OF EIf5A A method and pharmaceutical composition for inhibiting or preventing the intracellular biosynthesis of EIf5A by the administration to a human or non-human mammal in need thereof an amount of a polyamine analogue or salt thereof sufficient to deplete the supply of intracellular spermidine required for EIf5A biosynthesis.
CN101156870A A composition for improving growth development and help in improving anamnesis as well as its preparation method The invention relates to a composition which can improve growth and development and assist to improve memorization and the preparation method thereof. The invention is characterized in that the composition consists of lysine, taurine, retinol, aneurin, colecalciferol, riboflavin, DHA, folacin, zinc gluconate, ferrous gluconate, calcium carbonate, yeast, starch, stevioside, sucrose, nilk powder, citric acid, lemon yellow, and magnesium stearate. The preparation method comprises the following steps: raw materials are weighed according to the amount of formula, respectively pulverized with a universal pulverizer, after passing through a sieve of 80 meshes, the raw materials are mixed, the sucrose is dissolved in water to obtain 60 percent of molasses for backup, the lemon yellow is dissolved in the water, the molasses is poured into the water and uniform mixing is performed, then the mixture is mixed with the mixed powder of the other raw materials to produce soft material, wet granules are produced with a granulator, and after passing through a sieve of 18 meshes for drying, and then size stabilization and tabletting are performed. The invention has the advantages of improving the growth and the development and assisting to improve the memorization.
CN101327205A Use of lipoxin in treating tumor The invention provides a medicine for treating tumors. The medicine for treating tumor is Lipoxins and LXs. The LXs is used for treating tumors and has the functions of effectively restraining the reproduction of tumor cells, speeding up the death of tumor cells and restraining the spread of tumors.
CN1742812A Quick-acting antidiarrheic tablet and preparing method The present invention discloses a quick-acting antidiarrheal tablet and its preparation method. Said tablet is divided into general tablet and dispersing tablet. Every general tablet contains 80-160g of berberine hydrochloride, 100-250g of polygonum bistorta extract, 1-150mg of adhesive and 1-50mg of lubricating agent and flow aid, and every dispersing tablet contains 80-160g of berberine hydrochloride, 100-250g of polygonum bistorta extract, 1-200mg of filling agent, 10-200mg of disintegrant, 1-150mg of adhesive and 1-50mg of lubricating agent and flow aid.
CN102379894A Content determination method for montmorillonite preparation The invention relates to a content determination method for montmorillonite preparation. The content determination method is characterized in that montmorillonite powder is precisely weighed, the quantity of sampled montmorillonite powder is recorded, the sampled montmorillonite powder is placed in a centrifugal tube, 50% of ethanol or ethanol lower than 50% or water is added in the sampled montmorillonite powder by 20ml to 50ml, further, 10% to 20% of water-solubility salt liquor is also added in the sampled montmorillonite powder by one to two drops, after mixture of the sampled montmorillonite powder, 50% of ethanol or ethanol lower than 50% or water and 10% to 20% of water-solubility salt liquor is sufficiently shaken by 3000-5000 turns per fractional centrifugation for 10 minutes to 25 minutes, supernatant fluid is removed, the step is repeated by once to twice, then contents are transferred to an evaporation vessel with the constant weight, are evaporated and are dried at the temperature of 105 DEG C so that the weight of the contents is constant, and the weight of montmorillonite in tested substances is measured. The content determination method has the advantages that during centrifugation, the supernatant fluid is clear, loss of the montmorillonite is avoided when the supernatant fluid is removed, and accordingly, the content determination method is more accurate compared with an existing method.
CN103333157A Pyridine carboxamide derivative as kinase inhibitor The invention refers to a pyridine carboxamide derivative as a Kinase inhibitor. Specifically, New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
WO2014093383A1 Substituted 1h-pyrrolo [2,3-b] pyridine and 1h-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (sik2) inhibitors The present invention relates to compounds according to Formulas I, IA or IB: to pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.
CN101015603A Medicine composition with fat-reducing and bowel relaxing functions, preparing process and quality controlling means thereof The invention relates to a pharmaceutical preparation for fat-reducing and relaxing bowl, its preparing process and quality control method, wherein the preparation is made mainly from cassia seed, prepared rhubarb, sea tangle and chebula fruit through steps of disintegrating rhubarb horsetails, extracting other medicinal materials through ethanol backflow, concentrating, drying, collecting concrete powder, and mixing with rhubarb horsetails fines homogeneously to obtain clinically acceptable preparations. The quality control index of the composition is anthraquinones, whose content in unit preparation of 100g should be no lower than 300mg.
WO2012166859A2 Modulation of sphingosine 1-phosphate metabolizing enzymes for the treatment of negative-strand rna virus infections The present invention relates to compounds and methods for the prevention or treatment of infections by negative strand RNA viruses, such as influenza virus and measles virus, wherein said compounds delay or inhibit viral replication by modulating the level or activity of a polypeptide involved in the synthesis or degradation of sphingosine-1-phosphate (S1P) in a cell, tissue, or subject. The methods involve administration of one or more compounds which modulate the level of gene expression, where the gene encodes a polypeptide involved in regulating the metabolic level of S1P, or modulate the level or activity of a polypeptide involved in regulating the metabolic level of S1P, such as sphingosine kinase (SK) and S1P lyase (SPL). Exemplary methods are directed towards reducing the level of S1P by reducing the level or activity of one or more SKs, increasing the level or activity of one or more SPLs, or a combination of both steps.
US20120108629 New use of neferine The present invention reveals a new use of neferine. Neferine regulates M8 and V1 subtype of transient receptor potential ion channel (TRPM8 and TRPV1), respectively, in mammalians, including humans, and can be used for preparing medicaments for treating disease related to said ion channel (such as hyperalgesia, Parkinson's disease, painful bladder syndrome, chronic obstructive pulmonary disease, and tumor of skin, prostate, mammary gland, lung, colon, etc). The potency of neferine in the present invention is higher than that of hexahydrothymol.
EP2173362A2 Compositions and methods for inhibiting viral and bacterial activity Described herein are methods of inhibiting the activity of a virus or a bacterium comprising contacting a virus or bacterium with a polymer functionalized with at least one boronic acid moiety. Also described are methods of treatment using such functionalized polymers.
CN103301093A Testosterone transdermal absorbent patch The invention relates to a testosterone transdermal absorbent patch which consists of an anti-sticking layer, a drug-containing glue layer and a liner layer structure, and in particular relates to a compound type modifier formed by the combined action of a plurality of ingredients, so that the skin permeability and the medicine stability of the testosterone can be improved, and the prepared drug-containing glue layer is uniform and stable, more stable in a drug release process, and better in safety. The patch provided by the invention hardly falls off, and is easy to remove, and free from the phenomenon of glue residue during use process, thereby being good in clinic application prospect.
CN101816650A Ornidazole-sodium chloride combination and preparation method thereof The invention relates to an ornidazole-sodium chloride combination which is prepared from the following components according to the prescription: 5.0g of ornidazole, 8.5g of sodium chloride, a right amount of hydrochloric acid, and 1000 ml of water for injection. The preparation method of the combination comprises the following steps: dissolving the ornidazole and the sodium chloride in 1000ml of the water for injection, adding activated carbon with needle uses (0.05g/100ml) according to the proportion, decoloring by stirring at 25-50 DEG C for 20-30 minutes, standing for 15 minutes, filtering, adding the hydrochloric acid to adjust the pH to 4.5, sampling to measure the pH value and the content, fine-filtering by utilizing a sintered funnel and a microporous filtering film after conforming to the requirements, carrying out clarity detection, encapsulating after being qualified, and sterilizing at high temperature.
US20110165117 Immunogenic peptides and methods of use The PAGE4 gene is expressed in reproductive tissues, and is expressed in reproductive cancers, such as prostate cancer, uterine cancer, and testicular cancer. Immunogenic PAGE4 polypeptides are disclosed herein, as are nucleic acids encoding the immunogenic PAGE4 polypeptides, vectors including these polynucleotides, and host cells transformed with these vectors. These polypeptides, polynucleotides, vectors, and host cells can be used to induce an immune response to PAGE4. Diagnostic methods to detect PAGE4 are also described.
EP1303479B1 7-, 8- and 9-substituted tetracycline compounds 7,8 and 9-substituted tetracyline compounds of the formula (I) wherein: R?4 and R4'¿ are each methyl; R5 is hydrogen or hydroxyl; R?6 and R6'¿ are each independently hydrogen, methyl, or hydroxyl; R7 is hydrogen, lower alkenyl, lower alkynyl, phenyl, halophenyl, acyl, phenylalkynyl, heteroaryl, or dimethylamino; and R8 is hydrogen, phenyl, nitrophenyl, halo, or lower alkynyl; and R9 is hydrogen, amino, acetamide, or lower alkynyl; and provided that at least one of R?7, R8, or R9¿ is not hydrogen, methods of treating tretracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.
WO2006117181A3 Prophylaxis and treatment of diseases The invention relates to the use of at least one thiamine for the prophylaxis and/or treatment of diseases, which are associated with DNA lesions, whereby the administration of thiamine leads to a reduction in the DNA lesions.
CN101940785A Hydrogen sulfide-producing enzyme preparation and use thereof The invention discloses a hydrogen sulfide-producing enzyme preparation and use thereof. The preparation comprises the hydrogen sulfide-producing enzyme, 0.01 to 0.1 weight percent of pyridoxal phosphate and 0 to 0.1 weight percent of dithiothreitol, wherein the hydrogen sulfide-producing enzyme is enzyme capable of desulfurizing L-cysteine to produce hydrogen sulfide in the presence of trace amount of pyridoxal phosphate. The enzyme preparation can be mixed with conventional auxiliary materials to prepare an oral preparation, increases hydrogen sulfide supply, can treat and prevent diseases caused by suppressed production of endogenous hydrogen sulfide or insufficient production of endogenous hydrogen sulfide, and has the advantages of no toxic or side effect and wide application prospect.
WO2007075834A2 Use of benzo-fused heterocycle sulfamide derivatives for the treatment of epilepsy The present invention is a method for treating, preventing, reversing, arresting or inhibiting the occurrence, development and maturation of seizures or seizure-related disorders. More specifically, the present invention is directed to methods for the use of benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as described herein to therapeutically or prophylactically treat, prevent, reverse, arrest or inhibit epileptogenesis and epilepsy.
EP1922094A1 Methods and devices for lymphatic targeting The present invention is directed to an implantable device comprising a biocompatible and biodegradable matrix impregnated with a bioactive complex suitable for selectively targeting the lymphatic system, wherein the bioactive complex comprises one or more particle forming materials and one or more bioactive agents. The invention is further directed to methods of using and the process of preparing, the implantable device.
US7060730 Rapidly absorbed liquid compositions The present invention provides a method which provides for a faster absorption of pharmaceutically acceptable amines. The method provides a pharmaceutically acceptable amine in combination with a non-steroidal anti-inflammatory drug in a liquid form. A preferred embodiment employs pseudoephedrine and ibuprofen.
US8420108 Flexible bone composite The present invention relates in general to implantable flexible bone composites, and method for preparing the same. The flexible bone composite includes at least one polymeric layer and at least one calcium-containing layer. The polymeric layer can be a polymeric layer including a synthetic polymer. The calcium-containing layer can include a calcium compound such as β-Ca3(PO4)2. The flexible bone composites of the invention are useful as bone void fillers and have improved handling characteristics.
US20110183009 Mazindol Combination In The Treatment Of Attention-Deficit/Hyperactivity The present invention relates to the field of human health, and more particularly to the treatment of attention deficit/hyperactivity disorder (ADHD) with mazindol. The latter can be administered as monotherapy or in combination with one or more compounds, including psychostimulants, for the indication of ADHD and associated or co-morbid symptoms.
US20120129869 Phosphorylation and mutations of anaplastic lymphoma kinase as a diagnostic and therapeutic target in lung cancer The invention related to the use of high-density loss of heterozygosity (LOH) mapping in lung adenocarcinoma to identify intragenic LOH and driver mutations in different domains of ALK resulted in enhanced tumor growth in xenografted mouse. Mutant (H694R and E1384K) ALKs showed activation of Y1604 ALK and downstream AKT, STAT3 and ERK signaling pathways. Increases of oncogenic signalings resulted in enhanced cell proliferation, colony-formation, cell-migration and tumor-growth in xenografted mouse. Western blot and immunohistochemistry analysis using antibody against phospho-Y1604 ALK on 11 lung cancer cell-lines and 263 cancer specimens indicated ALK activation in all lung cancers regardless of tumor stages. Treating mutant-bearing mice with ALK inhibitor WHI-P 154 resulted in tumor shrinkage, metastasis suppression, and improved survival. Hyperphosphorylation of Y1604 ALK occurred early and continuously throughout tumor progression and could be used as a biomarker to detect lung cancer. Oncogenic ALK point mutations could be treatment targets for lung cancer.
US20070099904 Pharmaceutical composition for the treatment of cns and other disorders The present invention relates to compounds of formula I The substituent designations are as disclosed. At least one of B Q, D and E is nitrogen. The present invention also provides a method of treating disorders of the Central Nervous System such as schizophrenia and cognitive dysfunction.
CN103432583A Application of phthalocyanine and albumin composite in preparing sound-sensitive agent The invention discloses application of a phthalocyanine and albumin composite in preparing a sound-sensitive agent. The phthalocyanine and albumin composite has the advantages of high biocompatibility, high sonodynamic anti-cancer activity and the like while being used as a sound-sensitive agent for preparing a sonodynamic therapeutic drug.
CN101703657B External preparation for treating verruca vulgaris The invention discloses an external preparation for treating verruca vulgaris, and relates to an external preparation for treating verruca vulgaris, which comprises the following materials: 35 to 45g of rhubarb, 20 to 30g of baical skullcap root, 120 to 140g of common scouring rush herb, 85 to 95 grains of java brucea fruit, 38 to 46g of golden larch bark, 120 to 140g of dark plum fruit, 120 to 140g of nutgrass galingale rhizome, 85 to 95g of salicylic acid, 3 to 5g of podophyllotoxin, 90 to 110 milliliters of ethanol and 2,800 to 3,000 milliliters of dimethylsulfoxide. According to the pathogenesis and pathogenic factors of the verruca vulgaris, the rhubarb, the baical skullcap root and the common scouring rush herb are used for antivirus, antibiosis and antiphlogosis to strengthen the immune function; the java brucea fruit is used to resist pathogen and the proliferation of fibroblast and corrode warts; the salicylic acid is used to dissociate keratin; and the dimethylsulfoxide is used to embed the podophyllotoxin inhibiting the metakinesis of cells into focus. The external preparation has the advantages of little medication, concentrated potency of the medicaments, symptom and root cause addressing, quick medicinal effect, safety, reliability, convenient use and good curative effect. Clinical observation of 40 cases shows that the effective rate of the external preparation reaches 100 percent.
CN101317818A Methopterin intralipid, its freeze drying agent, preparation method and application thereof The invention relates to methotrexate intralipid, a freeze-dried agent, a preparation method and an application thereof. The methotrexate intralipid consists of methotrexate active ingredient, oil for injection, emulsifying agent, stabilizing agent, isotonic adjustment agent, antioxidant, amylose, water for injection and pH modifying agent. The methotrexate intralipid of the invention is freeze-dried to obtain the freeze-dried agent of the methotrexate intralipid. The methotrexate intralipid and the freeze-dried agent of methotrexate intralipid can be applied to the medicines for treating a tumor and rheumatoid diseases.
WO2014085958A1 Erythromycin derivatives and preparation and use thereof The erythromycin derivatives of the present invention, i.e., hydrated crystals of erythromycin stearate, has low moisture absorption and good storage stability, and is suitable for preparing drugs for treating and preventing infectious diseases in humans or animals caused by sensitive Gram-positive or Gram-negative bacteria, chlamydia or mycoplasma.
CN102125573A Use of ginsenoside Rg1 in preparation of antidepressant The invention belongs to the field of medicine and health and particularly relates to the use of a natural compound, namely a ginsenoside monomer Rg1, in the preparation of an antidepressant. A test dose of ginsenoside Rg1 can reduce dead time of a mouse in a tail suspension experiment and obviously reduce the dead time of a mouse in a forced swimming experiment and the times of escape failures of a mouse in a learned helplessness experiment, which shows that the ginsenoside Rg1 has a remarkable antidepressant effect and can be used for preventing and treating depression.
US7838020 Cosmetic or dermatological composition comprising an association between a compound of the N-acylaminoamide family and at least one matrix metalloproteinase inhibitor A cosmetic or dermatological composition characterized in that it comprises an association between an elastase inhibitor compound of the N-acylaminoamide family and at least one metalloproteinase inhibiting compound.
US20100278729 Breast cancer eradication program A method of treating breast cancer that is at least partially ER+ is disclosed. The method comprises administering at a tumor site in a mammalian subject a pharmaceutically acceptable form of Fe(II) or Fe(III) in a suitable carrier. A four-part program aimed at eradicating breast cancer includes (a) local treatment and prevention of spread from a contained breast site, preferably using local administration of a ferric iron composition, (b) treatment of disseminated (metastatic) breast cancer, (c) reduction in the risk of developing breast cancer, preferably by enhancing dimeric/polymeric IgA and polymeric IgM inhibition of estrogen responsive cell growth, and (d) protection against cancer causing agents.
CN103142647A Lanthanum hydroxide therapeutical effects on hyperphosphatemia and relative diseases The invention relates to lanthanum hydroxide which has the functions of preparing and curing chronic renal failure (CRF), hyperphosphatemia or/ and hyperparathyroidism (SHPT), vitamin D metabolic block, renal osteopathy and cardiovascular system calcification drugs, wherein the lanthanum hydroxide is nanometer lanthanum hydroxide, and daily dose of the lanthanum hydroxide or the nanometer lanthanum hydroxide is 600mg to 7800mg..
CA2411961C Novel process for the preparation of pyrazolopyrimidinones There is provided a process for the production of a compound of general formula (I) wherein A, A1, R2, R3 and R4 have meansings given in the description, which process comprises the reaction of a compound of formula (II), wherein Rx is a group substitutable by an aminopyrazole, with a compound of general formula (III).
US20090087443 Pharmacological Adjunctive Treatment Associated with Glaucoma Filtration Surgery A composition for controlling or preventing progression of glaucoma comprises a material that reduces or inhibits production of a TGF-β isoform or a chemokine or cytokine that stimulates expression of a TGF-β isoform. The material can comprise a dissociated glucocorticoid receptor agonist (“DIGRA”), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can further comprise an antagonist to TGF-β. It is administered to a patient who has undergone glaucoma filtration surgery to ensure a functioning filtering bleb following such surgery.
US20100144733 Compounds, compositions and methods comprising heteroaromatic derivatives The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-14 or encompassed by formulas I-XII) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
EP2083006A1 Oxadiazolones, processes for their preparation and their use as pharmaceuticals The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved; neurodegenerative diseases and/or demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuroinflammatory processes and/or other peripheral neuropathies.
CN102813675A Compound potassium hydrogen phosphate medicine combination for injection The invention discloses a compound potassium hydrogen phosphate medicine combination for injection. The compound potassium hydrogen phosphate injection is composed of monopotassium phosphate, dipotassium phosphate trihydrate and sodium calcium edentate, and each compound potassium hydrogen phosphate medicine combination for injection contains 435.4-870.8mg of monopotassium phosphate, 487.7-975.4mg of dipotassium phosphate trihydrate calculated by dipotassium phosphate, 1-2mg of sodium calcium edentate and injection water which is added for enabling the solution to be 2L-4L. A preparation method includes: taking 70% injection water with the amount described in the prescription at the temperature of 70 DEG C to 80 DEG C, and adding sodium calcium edentate with the amount described in the prescription, stirring the materials to be dissolved; adding the monopotassium phosphate with the amount described in the prescription and the dipotassium phosphate trihydrate with the amount described in the prescription calculated by dipotassium phosphate, stirring to enable the materials to be completely dissolved; measuring the original pH value, and regulating the range of the pH value to be 5.5-6.5 with 4% sodium hydroxide solution and 10% phosphoric acid solution; adding medicinal carbon for stirring; performing suction filtering, replenishing the injection water to the full dose, and evenly mixing; fine filtering; filling; sterilizing; performing lamp testing; and filling the combination in a warehouse to obtain the compound potassium hydrogen phosphate injection. The compound potassium hydrogen phosphate medicine combination is good in photostability, does not crystallize, is good in clarity and stability, improves product yield, reduces the cost, achieves industrialization, can be better applied to clinical use and has obvious advantages.
CN103159770A Crystal form of ertapenem monosodium salt The invention provides a crystal form of ertapenem monosodium salt. In a powder X-diffraction pattern of the crystal form, characteristic peaks exist in positions where the diffraction angle 2theta is 4.1+/-0.1, 4.8+/-0.1, 6.8+/-0.1, 7.9+/-0.1, 10.4+/-0.1, 11.7+/-0.1, 13.6+/-0.1, 14.4+/-0.1, 18.6+/-0.1, 19.6+/-0.1, 21.5+/-0.1, 22.0+/-0.1, 23.9+/-0.1, 24.1+/-0.1, 26.9+/-0.1, 27.4+/-0.1 and 31.1+/-0.1. According to the invention, the crystal form of ertapenem monosodium salt has favorable stability; and the preparation method is simple to operate, high in yield, low in cost and suitable for industrial production.
EP0756005B1 Gene coding for adseverin A DNA containing a base sequence coding for the amino acid sequence represented by SEQ ID NO: 4 or 5, a base sequence derived from the above sequence through partial substitution, deletion or addition, or a base sequence which hybridizes with them; a recombinant vector containing said gene; a transformant prepared with said vector; a process for producing adseverins; a recombinant adseverin protein produced by the above process; an oligonucleotide hybridizable with a base sequence coding for the amino acid sequence represented by SEQ ID NO: 4 or 5; a method of suppressing adseverin formation in animals by administering said oligonucleotide thereto; and an antibody recognizing adseverin proteins.
WO2008059224A1 Use of buprenorphine or n-alkylated derivatives thereof for wound healing This invention relates to opioid compounds such as burenorphine or N-alkylated derivatives thereof for wound healing.
US20090148546 Methods and compounds fo rthe treatment of obesity and obesity-related disorders In certain embodiments, the invention comprises the use of plant-derived substances to reduce body fat and/or to increase insulin sensitivity in mammals. In certain embodiments, the invention comprises a composition for reducing the amount of fat in the body of a mammal, the composition comprising at least one plant-derived substance which inhibits adipogenesis in the body of the mammal and at least one plant-derived substance which promotes lipolysis in the body of the mammal. In certain embodiments, the invention comprises a composition for reducing the amount of fat in the body of a mammal, the composition comprising at least one plant-derived substance which inhibits adipogenesis in the body of the mammal, at least one plant-derived substance which promotes lipolysis in the body of the mammal, and at least one plant-derived substance which inhibits lipogenesis in the body of the mammal. In certain embodiments, capsaicin may be used in combination with other plant-derived substances to reduce the body fat in a mammalian subject. In one embodiment, an effective amount of a composition comprising capsaicin in combination with grape seed extract and/or genistein and/or caffeine may be administered to a subject to reduce the body fat of the subject. In one embodiment, a composition comprising grape seed extract is administered to a mammalian subject to increase insulin sensitivity.
US20110182963 Osteoimplant and methods for making An osteoimplant is disclosed and includes a plurality of partially demineralized fibers. Each fiber has an elongated, thin body having a length of about 1 centimeter to about 3 centimeters. Further, the plurality of fibers engages to establish a matrix of material. The disclosure is further directed to a method of making the above-mentioned osteoimplant.
US20050176806 Use of 1-[3-hydroxy-1-adamantylamino]acetyl-2-cyano-pyrrolidine, for example with other anticholesterol drugs such as statins Disclosed are methods and compositions for the treatment of hyperlipidemia and conditions associated therewith, such as CHD, ischemic stroke, restenosis after angioplasty, peripheral vascular disease, intermittent claudication, myocardial infarction (e.g. necrosis and apoptosis), dyslipidemia and post-prandial lipemia. The methods include administration of a therapeutically effective amount of a compound of formula I wherein R is substituted adamantyl; and N is 0 to 3; in free form or in acid addition salt form, and a pharmaceutically acceptable carrier.
EP2403517A1 Novel antiviral agent The present invention relates the use of a composition including or consisting of at least one element selected from among: a predetermined protein including or consisting of the amino acid sequence SEQ ID NO: 5, and a homologous protein of said predetermined protein, for preparing a drug for preventing or treating diseases related to a viral infection or inflammation.
WO2010014888A3 Use of a pneumococcal p4 peptide for enhancing opsonophagocytosis in response to a pathogen Methods for enhancing opsonophagocytosis of a pathogen of interest are disclosed. The disclosed methods include administering to a subject an isolated P4 peptide, which including the amino acid sequence set forth as SEQ ID NO: 1 and optionally an isolated opsonic antibody or a fragment thereof that specifically binds to an antigen present of the surface of the pathogen of interest. In some examples isolated complement protein or a fragment thereof (for example, a C3a, C3b, iC3b, C3d, C4b, or C5a fragment of a complement protein) is also administering. Compositions contain isolated P4 peptide and one or more isolated opsonic antibodies or a fragment thereof that specifically binds to an antigen present of the surface of a pathogen of interest are also disclosed. In some examples, the compositions also isolated complement protein or fragment thereof, such as one or more of C3a, C3b, iC3b, C3d, C4b, or C5a.
US20110166094 Agonists of a2a adenosine receptors for treating recurrent tumor growth The present invention relates to a method for treating recurrent tumor metastases following liver resection that includes administration of an effective amount of an agonist of A2A adenosine receptors (ARs).
US20110038921 Methods and compositions for temporal release of agents from a biodegradable scaffold The present invention provides methods and compositions for sequentially and separately reducing infection and/or inflammation and regenerating tissue at a lesion site, by contacting the lesion site with a biodegradable scaffold that first delivers one or more agents at the lesion site to reduce infection and/or inflammation and then delivers one or more agents to regenerate tissue at the lesion site after inflammation is reduced.
CN102068572A Pedate pinallia jackinthepulpit rhizome externally applied preparation for treating bruises The invention relates to a pedate pinallia jackinthepulpit rhizome externally applied preparation for treating bruises, which can effectively solve the medication problem for treating the bruises. The technical scheme for solving the problem is as follows: the preparation is prepared by mixing pedate pinallia jackinthepulpit rhizome medicinal powder with rice vinegar or white spirit, wherein pedate pinallia jackinthepulpit rhizome medicinal material is smashed and passes through an 80-120-mesh sieve for forming the pedate pinallia jackinthepulpit rhizome medicinal powder, then the medicinal powder and the rice vinegar or the white spirit are blended into paste, and 0.15-0.25g of the medicinal powder is added into each milliliter of the rice vinegar or the white spirit. The rice vinegar is one type of vinegar, which is liquid containing acetic acid brewed from rice and has the effects of removing blood stasis, stopping bleeding, removing toxin and killing ascarid. The white spirit is commercially available white spirit with mass concentration of 40-65 degrees. The pedate pinallia jackinthepulpit rhizome externally applied preparation has abundant raw materials, low production cost, convenience in application and high efficacy, and is an innovation in externally applied medicaments for treating the bruises.
US20120016003 Pot1 alternative splicing variants The present invention provides methods and compositions for diagnosis and treatment of carcinomas with aberrant expression patterns of POT 1. The invention also provides methods of identifying compounds that may modulate the cellular expression of POT 1. The invention further provides methods for treating subjects suffering from or at risk of developing a colorectal carcinoma.
US7976860 A porous protein matrix with a structural component partly or fully anchored in the matrix; at least one surface has a protein membrane crosslinked with the matrix; sufficient stability with improved flexibility, biocompatibility and absorption; vascular prosthetics The present invention relates to an implant having a structured material component and having a protein matrix which has a pore structure. The structured material component is moreover at least partly anchored in the protein matrix. The implant also has on at least one its surfaces a protein membrane crosslinked with the protein matrix.
CA2304770C A use of steroidal saponins for the prophylaxis or treatment of dementia, and novel steroidal saponin compounds The invention relates to the steroidal saponin compounds for the prophylaxis or treatment dementia, the new steroidal saponin compounds and the pharmaceutical composition containing the same.
EP2099800A1 7-substituted purine derivatives for immunosuppression The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula (III).
CN102432592A Aryl urea derivate having anti-tumor function and preparation method of aryl urea derivate The invention discloses an aryl urea derivate which is structurally represented by a general formula I, and belongs to the field of pharmaceutical chemistry. Substituent groups in the general formula I are defined in the specification. The invention also discloses a preparation method of a compound of the general formula I. The compound has the function of an raf kinase inhibitor and can be applied to preparation of drugs for treatment of tumor diseases.
WO2014149280A1 Treatment of pets with sirtuin activators The present invention provides for systems, compositions, methods and kits for regulating energy metabolism in pets. The systems, compositions, and kits can comprise, and methods can make use of, pet foods, pet treats, pet supplements, and pet drinks. In one aspect, the invention provides for pet food, treat, supplement, and drink compositions that comprise a combination of (a) leucine, and (b) a sirtuin activator, or any precursors or metabolites of (a) or (b). These combinations may be effective for reducing weight or adipose volume in the pet. In another aspect, the invention provides for methods of regulating energy metabolism by the administration of one or more compositions comprising leucine, a leucine metabolite, and/or a sirtuin activator. The invention also provides for kits comprising compositions of leucine, a leucine metabolite, and/or a sirtuin activator packaged in an oral dose form with usage instructions.
CN1900078A Entecavir potassium salt compound and its preparing method and medicine use The present invention relates to entecavir potassium salt compound and its preparation process and application in preparing medicine. Entecavir potassium salt is prepared through dissolving entecavir in the water solution of potassium hydroxide to react with potassium hydroxide, precipitating with low carbon chain single alcohol or ketone, and drying. Entecavir potassium has excellent water solubility, is used as material medicine, and can result in high medicine bioavailability.
EP2460787A1 Amide compounds and their use as PGE2 antagonists. [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.
US20100249045 Multimodal Abuse Resistant and Extended Release Opioid Formulations The present invention is in the field of oral, abuse resistant pharmaceutical compositions of opioid agonists, extended release pharmaceutical compositions of opioid agonists and extended release abuse resistant pharmaceutical compositions of opioid agonists and the use thereof. The present invention is also directed to extended release pharmaceutical compositions and the use thereof for preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering. The present invention is further directed at a method of preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering.
CN101756924A Sustained-release tablets of faropenem sodium The invention belongs to the field of Western medicine preparations, in particular to sustained-release tablets of faropenem sodium. The sustained-release tablets consist of the faropenem sodium, sustained-release materials and other excipients, wherein the sustained-release materials account for 5-50% of the weight of the preparation; preferentially, the sustained-release materials account for 10-30% of the weight of the preparation. The sustained-release tablets can reduce the dosing times, avoid or reduce the peak-valley phenomenon of the plasma drug concentration, provide the smooth and lasting effective plasma drug concentration and improve the safety and the effectiveness of a drug.
CN101156852A Lansoprazole intestine solution capsule and its preparation method The invention discloses a lansoprazole enteric liquid capsule which has a simple manufacturing process, avoids water from being led in during the manufacturing process, and has good storage stability and a manufacturing method. The lansoprazole enteric liquid capsule consists of lansoprazole, dispersant, edible vegetable oil, magnesium oxide or magnesium carbonate, an emulsifier, poloxamer, animal and vegetable glue, and sodium citrate. After being mixed uniformly, raw materials enter into a colloid mill, and then the raw materials are infused into a hollow capsule, and polyacrylic resin ethanol solution is used as the sealing material to sleeve and seal the infused capsule. The invention suspends the lansoprazole into hydrophobic excipient oil, forms a protective film around the lansoprazole powder, does not lead in water during the manufacturing process, avoids the degradation of the lansoprazole, does not need to wrap an isolation layer and an enteric coating, and has short production cycle, simple production process, low cost, and good product quality and stability.
US20100075940 Dendritic polyamidoamine phthalocyanine derivative The present invention is directed to a dendritic polyamidoamine phthalocyanine derivative which is useful as, for example, a fluorescent material or a photodynamic therapeutic drug for cancer. The derivative is represented by the following formula (1): (wherein each member of one to eight of R1 to R8 is a polyamidoamine dendron represented by the following formula (a): (wherein p is a number from 1 to 4; R9 represents —NH(CH2)NH2 or OR10 (wherein R10 represents an alkyl group); and each of l, m, q, and t is a number from 1 to 8), and each member of the remainder represents a hydrogen atom; M represents a metal atom having a valency of two or more; and a ring marked with (N) is a benzene ring, a pyridine ring, or a pyrazine ring).
CN103565808A Application of dexlansoprazole in preparation of drug for treating hemorrhagic digestive tract diseases The invention relates to a novel application of dexlansoprazole in the pharmaceutical field, specifically relates to application of dexlansoprazole in preparation of a drug for treating hemorrhagic digestive tract diseases, and particularly relates to application of the dexlansoprazole in preparation of a drug for treating hemorrhagic gastric ulcer, duodenal ulcer, acute stress ulcer and acute gastric mucosal lesion which are inapplicable to an oral-taking therapy. Experimental result proves that pharmacodynamic activity of the dexlansoprazole is remarkably higher than that of lansoprazole levo form, and higher than that of racemate, and therefore the dexlansoprazole is a main active ingredient of lansoprazole, which takes effect in body, and is capable of lowering clinical use dosage and lowering potential toxic and side effects when used independently. The dexlansoprazole used in the invention is a single active ingredient with material purity being higher than 99.5%, and can effectively avoid toxicity risks caused by other impurities in the drug; therefore, drug use is safe, drug quality is more controllable, and curative effect is more exact.
EP2338889A1 Diazacyclic compounds having affinity for opioid receptors Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1 (I) wherein: - A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R', C(O)OR', C(O)NHR' or C(O)NR3R4, R', R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted - D1 is a diazapolycyclic group - T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.
CN103588892A Solvent extraction method for active polysaccharide of wheat bran The invention discloses a method for extracting active polysaccharide-araboxylan from wheat bran through a compound solvent. The extraction method mainly comprises the following steps: the wheat bran is mildly hydrolyzed and preprocessed by a weak acid (citric acid); the target polysaccharide is extracted through a strong alkali (KOH); the extracting solution is centrifugated, neutralized, concentrated and subjected to ethanol precipitation; the ethanol precipitate is dried to obtain the target polysaccharide. The centrifuged supernate of the ethanol precipitate is concentrated and dried, and then can be used as an agricultural compound fertilizer for comprehensive utilization. According to the invention, a large quantity of the byproduct resource, namely the wheat bran is utilized, and the compound solvent is designed to extract the biological active polysaccharide, namely the araboxylan. Compared with the traditional alkali method, the extraction method improves the working efficiency, and reduces the environmental protection pressure. Animal experiments prove that the polysaccharide has prominent immunoregulatory activity, and the effect is comparable to that of lentinan. According to the target polysaccharide provided in the invention, the raw material is low in cost and rich, and the extraction method is environment-friendly, so that the industrialization development of the polysaccharide is promising in the future.
US20070254888 Piperazinediones as Oxytocin Receptor Antagonists Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
CN102627682A Esterified and halogenated stigmasterol derivate and application thereof in anti-cancer drugs The invention discloses an esterified and halogenated stigmasterol derivate and an application thereof in anti-cancer drugs. The chemical structure formula of the esterified and halogenated stigmasterol derivate is shown as follows: in the formula, the group represented by R1 is as defined in the specification. The in-vitro cancer cell inhibition test shows that the esterified and halogenated stigmasterol derivate has a remarkable inhibition effect on various tumor cells such as a human breast cancer cell strain (MCF-7), a human lung cancer cell strain (A549) and a human liver cancer cell strain (HepG2) and the like, wherein the inhibition effect of a compound 3 on the three cancer cells is equivalent to and even is superior to that of a positive contrast. The esterified and halogenated stigmasterol derivate can be used for preparing the anti-cancer drugs.
US20130150436 Polyacetylene compound, an extract containing the same and application thereof A polyacetylenes and application thereof. The polyacetylenes is isolated from an extract of the sporophores of Antrodia Cinnamomea and has a function of inhibiting the production of nitric oxide. Therefore, the polyacetylenes can be used for preparing a pharmaceutical composition for anti-inflammation. The present invention also teaches the representative metabolites of the sporophores of Antrodia Cinnamomea, which can be used to evaluate the quality thereof.
CN101690802A Cervical mucosa inducing gel The invention relates to a gel which can improve vaginal microenvironment and restore vaginal microdamage and is suitable for treatment on various kinds of vaginitis and cervicitis caused by vaginal microecological disturbance and vaginal microdamage, auxiliary treatment on vaginitis and cervicitis after clinical treatment, and treatment on cervical erosion, in particular to a cervical mucosa inducing gel which comprises carbomer, triclosan and human epidermal growth factors, wherein the concentration of the carbomer is 3%-5%, the concentration of the triclosan is 0.1%-0.6%, and the concentration of the human epidermal growth factors is 1/100000-1/10000. The cervical mucosa inducing gel can effectively improve the vaginal cleanness and increase the lactobacillus quantity to further reduce the vaginal pH value, has obvious effect on restoring cervical erosion, and can be used for auxiliary treatment on vaginitis and cervicitis after treatment.
WO2005011682A1 Sustained release tablet for oral use [PROBLEMS] To provide a sustained release tablet for oral use which causes no rapid increase in the concentration of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) in the blood at the early stage of the administration and makes it possible to maintain an appropriate concentration thereof in the blood over a long period of time. [MEANS FOR SOLVING PROBLEMS] A sustained release tablet for oral use characterized by being obtained by adding a gel-forming substance to a medicinal composition containing KRP-197 as the active ingredient.
EP1137635B1 N-substituted 2-cyanopyrrolidines The present invention relates to a compound of formula (I), wherein R is substituted adamantyl; and n is 0 to 3; in free form or in acid addition salt form. Compounds of formula (I) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
EP1503737A1 Nanoparticulate nystatin formulations The present invention is directed to nanoparticulate compositions comprising nystatin. The nystatin particles of the composition have an effective average particle size of less than about 2000 nm.
CN102120022B Medicament for treating pain and fever caused by cancer The invention discloses a medicament for treating pain and fever caused by cancer. The medicament comprises the following bulk pharmaceutical chemicals in parts by weight: 0.015-0.04 part of diclofenac sodium, 0.00075-0.0015 part of dexamethasone, 0.001-0.002 part of cyproheptadine, 10-20 parts of Indian iphigenia bulb, 8-15 parts of vietnamese sophora root, 10-30 parts of Sculellaria barbata, 10-18 parts of Chinese lobelia, 7-16 parts of Pinellia ternate, 5-15 parts of rhizoma sparganii, 10-30 parts of curcuma zedoary, 10-25 parts of cinnamon, 5-25 parts of ginseng, 15-30 parts of lucid ganoderma and 20-40 parts of liquorice. As the bulk pharmaceutical chemicals are combined, the medicament disclosed by the invention achieves obvious analgesic and pyretolysis effects clinically, has goodtreatment effects on serious pain caused by terminal cancer and fever which can not be cured for a long time, and is not addictive to patients, therefore, the medicament can be taken for long time. The medicament disclosed by the invention has the advantages of good analgesic and pyretolysis effects, low dosage, rapid response and low toxicity, and can be taken conveniently; and the bulk pharmaceutical chemicals can be easily obtained.
CN102127097A N-(3S-1, 2, 3, 4- tetrahydroisoquinoline-3-formoxyl) cupric amino-acid complex, preparation method and application of complex The invention discloses an N-(3S-1, 2, 3, 4- tetrahydroisoquinoline-3- formoxyl) cupric amino-acid complex, a preparation method and an application of the complex as an antithrombotic agent. The N-(3S-1, 2, 3, 4- tetrahydroisoquinoline-3-formoxyl) cupric amino-acid complex with antithrombotic activity is prepared from N-(3S-1, 2, 3, 4- tetrahydroisoquinoline-3-formoxyl) amino acid with antithrombotic activity, and the functions of the N-(3S-1, 2, 3, 4- tetrahydroisoquinoline-3-formoxyl) cupric amino-acid complex which is taken as the antithrombotic agent and platelet aggregation inhibitor can be further evaluated on an animal model.
US20100021394 High penetration prodrug compositions of 1h-imidazo[4,5-c]quinolin-4-amines and 1h-imidazo[4,5-c]quinolin-4-amine-related compounds The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of 1H-imidazo[4,5-c]quinolin-4-amines and 1H-imidazo[4,5-c]quinolin-4-amine-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
WO2008080120A3 3-amino chromane derivatives The present invention relates to 3-amino chromane derivatives; to compositions containing such compounds; to methods of synthesizing such compounds; and to methods of using such compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety.
US20100130614 ADMINISTRATION OF ADAPALENE FOR MODULATING THE EXPRESSION OF IL-1ra Adapalene or pharmaceutically acceptable salt thereof is administered to an individual in need of such treatment for modulating the expression of IL-1ra by the cells of acneic epidermis.
US20100168118 Methods to Treat Cancer with 10-propargyl-10-deazaaminopterin and Methods for Assessing Cancer for Increased Sensitivity to 10-propargyl-10-deazaaminopterin The present invention relates to a method for assessing the sensitivity of a patient's cancer to treatment with 10-propargyl-10-deazaminopterin and a method for selecting a patient for treatment of cancer with 10-propargyl-10-deazaminopterin, by determining the amount of a selected polypeptide expressed by the cancer and comparing the amount with the amount of the selected polypeptide expressed by a reference cancer, wherein the polypeptide includes a member of folate pathways within cells and may include at least one of reduced folate carrier-1 enzyme (RFC-1), dihydrofolate reductase (DHFR), folylpoly-gamma-glutamate synthetase (FPGS), thymidylate synthase (TS), γ-glutamyl hydrolase (GGH), and glycinamide ribonucleotide formyltransferase (GARFT). The present invention also relates to the use of 10-propargyl-10-deazaminopterin in the treatment of multiple myeloma.
WO2014097875A1 Development of pluripotent stem cell employing novel dedifferentiation induction method The purpose of the present invention is to obtain: a novel pluripotent stem cell production method; or a therapeutic agent for malignant tumors. A method for inducing the dedifferentiation of a cell, which involves a step of inhibiting the expression or function of a miR-520d-5p-controlled gene, is employed. Or, a therapeutic agent for malignant tumors, which comprises an inhibitor of the expression or function of the miR-520d-5p-controlled gene, is used.
US20080221065 Pharmaceutical formulations; epothilone and mannitol or a cyclodextrin parenteral administration in the form of an infusion concentrate or lyophilised composition Pharmaceutical formulations comprising an epothilone in the form of an infusion concentrate or a lyophilised composition, and methods of administration of an epothilone in suitable form for parenteral administration.
US7781470 Aminodicarboxylic acid derivatives having pharmaceutical properties The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.
US20100093657 Low glycemic mixtures The present invention relates to a food compound comprising an emulsion containing triglyceride oils as well as a low-glycemic saccharose isomer.
US20120040923 Stable s-adenosyl-l-methionine Stable compositions of defined non-racemic diastereomeric ratios of S-adenosyl-L-methionine, methods for their synthesis and methods for their uses are described. The compositions according to the invention are very stable and are valuable for use as active constituents in pharmaceutical compositions.
WO2012025123A1 Therapeutic uses of 1-[2-(2,4-dimethyl-phenylsulfanyl)phenyl]piperazine The invention provides new therapeutic uses of 1-[2-(2,4-dimethyl-phenylsulfanyl)phenyl]- piperazine and pharmaceuticallyacceptable salts thereof.
US20110281888 Fused Bicyclic Kinase Inhibitors Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.
WO2014126266A1 Difluprednate emulsion composition containing zinc The present invention relates to an emulsion composition containing difluprednate and zinc. The present invention also relates to a method of stabilizing an emulsion composition containing difluprednate, the method includes preparing an emulsion composition comprising difluprednate and zinc. According to the present invention, a difluprednate-containing emulsion composition having excellent preservative efficacy and excellent stability (photostability and heat stability) can be provided.
WO2013104257A1 Polycyclic derivatives, preparation method and medical uses thereof Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutical agents, especially the GPR40 agonist and in preparation of drugs for treating diseases like diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.
EP2433636A1 Treatment of Malignant Diseases The invention discloses a compound selected from the group N*2*,N*4*-Bis-(2-methyl-1H-indol-5-yl)-pyrimidine-2,4-diamine, N*2*-(4-Diethylamino-1-methyl-butyl)-5-methyl-N*4*-(2-methyl-1H-indol-5-yl)-pyrimidine-2,4-diamine, N*2*,N*4*-Bis-(1H-indol-5-yl)-pyrimidine-2,4-diamine and N*2*-(1H-Indol-6-yl)-N*4*-(1H-indol-5-ylmethyl)-pyrimidine-2,4-diamine, preferably N*2*,N*4*-Bis-(2-methyl-1H-indol-5-yl)-pyrimidine-2,4-diamine, and any of its stereoisomeric forms or a mixture thereof; or a salt or solvate of a compound of these compounds, especially for use in the treatment of malignant diseases.
CN102872098A Application of Houttuynoid A in medicine for preventing and treating renal insufficiency The invention discloses application of Houttuynoid A in a medicine for preventing and/or treating renal insufficiency, belonging to the technical field of new application of a medicine. The application of Houttuynoid A in preparing a medicine for preventing and treating renal insufficiency is disclosed for the first time; and since the skeleton type is a brand new one and the activity in suppressing renal insufficiency is unexpectedly strong, the possibility of any other compound offering any inspiration does not exist, outstanding substantial characteristics are obtained, and an obvious progress is made in preventing and treating renal insufficiency.
US20050070595 Complex of trioxane with iron compound This application relates to compounds of the general formula (11), and pharmaceutically acceptable salts thereof, in which R is selected from the group comprising optionally substituted alkyl, aryl, bisalkyl or bisaryl ester, bisalkyl or bisaryl ether, acetal, ketal, boronate, silyl ether, carbamate, carbonate, sulphate, sulphonate, phosphate and phosphonate, and to processes for their production. The compounds are useful as medicaments, in particular for the treatment of malaria and cancer.
CA2803656A1 Combination of glyt1 compound with antipsychotics The present invention relates to a pharmaceutical combination of a glycine transporter inhibitor (GlyT1) and an atypical antipsychotic drug which may be used for the treatment of positive and negative symptoms of schizophrenia.
CN103156844A Application of Schiff base compound in inhibition of activity of NDM-1 The invention provides application of a Schiff base compound in preparation of a medicine used for inhibiting activity of drug-resistant bacteria, especially in preparation of a medicine used for inhibiting activity of drug-resistant bacteria generating NDM-1. The Schiff base compound has a structural general formula (I) as described in the specification; in the general formula (I), an A ring is an aromatic ring group or a hetero-aromatic ring group, a B ring is an aromatic ring group or a hetero-aromatic ring group, R1 is selected from the group consisting of hydrogen, a hydroxyl group, a halogen, a C1-C4 alkyl group, a C1-C4 halogenated alkyl group, a C1-C4 alkoxy group and a nitro group, R2 is selected from the group consisting of hydrogen, a hydroxyl group, a halogen, a C1-C4 alkyl group, a C1-C4 halogenated alkyl group, a nitro group, a benzoyl group, a C1-C4 alkylamido group and an aryloxy group, and X represents inexistence or a methylene group or an ethylidene group. The Schiff base compound has the effect of inhibiting activity of NDM-1.
CN101283988A Danazol vaginal tablet process and quality control method The invention relates to a preparation method and a quality control method of a new drug, Danazol Vaginal Tablets, for treating endometriosis with clear dysmenorrhea symptom but light physical sign. The drug can be delivered via cavitary mucosa, so as to prevent or relieve the possible adverse reactions due to systemic drug delivery; the effective drug concentration at lesion site is high, so as to be in favor of exert curative action; and the added lactic acid-calcium lactate buffer system results in the drug with pH of 3.5-4.0 that is similar to the physiological pH in vagina, so as to effectively retain physiological environment in vagina, provide existing conditions suitable for vaginal beneficial bacteria, and promote rehabilitation.
WO2012007006A1 Triazolo- and pyrazoloquinazoline derivatives as pde10a enzyme inhibitor The invention relates to compounds of the formula (I) and their use as pharmaceutical ingredients, in particular for the treatment of CNS related diseases.
WO2011017634A2 Prodrugs of fused heterocyclic inhibitors of d-amino acid oxidase The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective.
WO2011080751A2 α4β2 NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS The present invention relates to novel α4β2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them. The present invention relates to novel α4β2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them.
US20120283325 Excipient compatibility with ezatiostat Disclosed herein is the surprising and unexpected discovery that mannitol inhibits the growth of impurities and enhances shelf life of ezatiostat hydrochloride formulations.
CN102020671A Preparation and application of 3,7,10-trimethyl-silatrane Schiff base derivatives The invention relates to a group of 3,7,10-trimethyl-silatrane Schiff base derivatives, and preparation and application thereof. The preparation method comprises the following steps of: reacting triisopropanolamine with gamma-aminopropyltriethoxysilane to obtain a gamma-amino propyl-3,7,10-trimethyl silatrane intermediate; and then performing a nucleophilic addition reaction of the gamma-amino propyl-3,7,10-trimethyl silatrane intermediate and different substituent-containing aldehyde in benzene solvent to obtain the 3,7,10-trimethyl-silatrane Schiff base derivatives. The 3,7,10-trimethyl-silatrane Schiff base derivatives have high plant growth regulating activity and high anti-inflammatory activity and can be applied to the preparation of a plant growth regulating agent and a cyclooxygenase (COX) inhibitor. The formula is shown as (I) in the specification.
CN102499914A Drug for treating strokes The invention relates to a drug for treating or preventing strokes or other neurological diseases/disorders by using inhibitors with inflammation-associated proteins. The drug has an important clinical application prospect.
US7135477 Administering N-(2-[N',N'-diethylamino]-5-[N''-(4-fluorophenylsulfonyl)-N''-propargylamino]pyrimidin-4-yl)-4'-(pyrrolidin-1-ylcarbonyloxy)-L-phenylalanine as an antiinflammatory agent treating rheumatoid arthritis Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
CA2402431C 1,2,3,4-tetrahydroisoquinoline derivatives The invention relates to novel 1,2 3,4-tetrahydroisochi-noline derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
WO2010097410A1 Novel bronchodilating diazaheteroaryls The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.
US20120269891 Controlled release oral pharmaceutical dosage forms comprising mgbg Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.
US7872125 1-Methyl,3-((1,3-dichloro-phenyl)-carbonylamino-(1-carboxy- eth-1,2-ylene)-(1,4-phenylene)-)quinazolin-2,4-dione; inhibiting the adhesion of VCAM-1 (vascular cellular adhesion molecules-1) to alpha-4 integrin; antiinflammatory agents; cardiovascular disorders; multiple sclerosis; antiarthritic agent Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
US8691785 Compositions and methods for non-parenteral delivery of oligonucleotides The present invention relates to compositions and methods which enhance the local and systemic uptake and delivery of oligonucleotides and nucleic acids via non-parenteral routes of administration. Pharmaceutical compositions comprising oligonucleotides disclosed herein include, for systemic delivery, emulsion and microemulsion formulations for a variety of applications and oral dosage formulations. It has also surprisingly been discovered that oligonucleotides may be locally delivered to colonic sites by rectal enemas and suppositories in simple solutions, e.g., neat or in saline. Such pharmaceutical compositions of oligonucleotides may further include one or more penetration enhancers for the transport of oligonucleotides and other nucleic acids across mucosal membranes. The compositions and methods of the invention are utilized to effect the oral, buccal, rectal or vaginal administration of an antisense oligonucleotide to an animal in order to modulate the expression of a gene in the animal for investigative, therapeutic, palliative or prophylactic purposes.
WO2010006121A3 19-nor-vitamin d analogs with 3,2-dihydrofuran ring 19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 3β-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro and in vivo activities, making them therapeutic agents for the treatment or prophylaxis of autoimmune diseases, some types of cancers, metabolic bone diseases, osteomalacia, osteopenia, secondary hyperparathyroidism, psoriasis, or other skin diseases.
EP1476192B1 Methods and compositions for treating hyperproliferative conditions The present invention relates to a combination which comprises (a) an inhibitor of a tissue non-specific growth factor receptor and (b) an inhibitor of a tissue specific growth factor receptor for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of phyperproliferative conditions, such as in particular cancer, in a mammal, particularly a human. The invention also relates to pharmaceutical compositions comprising such a combination and to a method of treating hyperproliferative conditions, such as especially cancer, with such a combination. The present invention further also relates to a commercial package or product comprising such a combination.
CN102335166A Pharmaceutical composition containing arctigenin and its application The invention relates to a pharmaceutical composition containing arctigenin and an application of the pharmaceutical composition in preparing medicine for treating cancer, especially an application of the pharmaceutical composition in preparing medicine for treating leukemia. The pharmaceutical composition of the invention comprises the active components arctigenin and all-trans retinoic acid. Preferably, according to an amount of substance, in the pharmaceutical composition of the invention, the mol ratio of arctigenin to all-trans retinoic acid is 1:0.01-100. In the pharmaceutical composition, the combination of the active components arctigenin and all-trans retinoic acid has synergetic effect for anti-leukemia.
CN102302483A Application of flavonoid small molecule medicine in anti-inflammation and associated diseases The invention discloses novel application of a flavonoid small molecule medicine (comprising naringenin, hesperetin, luteolin, apigenin and the like) in preparing a medicine for anti-inflammation and diseases associated with inflammation through illustrating a regulation mechanism of associated inflammatory cytokines and a regulation mechanism of the intracellular molecular level for a flavonoid small molecular compound in inflammatory response. The diseases associated with inflammation comprises: solid tumors (including lung cancer, liver cancer and breast cancer) with high metastatic potential, systemic organs fibrosis (including lung fibrosis, liver fibrosis), lung injury caused by concurrent chemoradiotherapy, lung fibrosis caused by concurrent chemoradiotherapy, and the like.
US7482363 N-[[4-(2-Chloro-4-fluorophenoxy)[1,4'-bipiperidin]-1'-yl]carbonyl]-4-methyl benzenesulfonamide, used for prophylaxis of respiratory system disorders or as antiallergens The present invention provides a compound of formula (I), wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
CN103230426A Medical composition for treating diabetes mellitus and complications thereof The invention provides berberine and panax notoginseng saponins and use of a composition using berberine and panax notoginseng saponins as effective components in preparing medicines for preventing and treating diabetes mellitus and complications thereof. The complications of diabetes mellitus are selected from diabetic cardiac abnormalities, diabetic renal lesions, diabetic retinopathy, diabetic peripheral neuropathy and diabetic vasculopathy.
CN101385719B Osmotic pump preparation composition for treating hyperlipemia The invention provides a new osmotic pump controlled-release pharmaceutical composition for treating hyperlipemia and a preparation method thereof, one of which is a nicotinic acid drug of acipimox, the other drug is a statin drug of pravastatin sodium, the acipimox and the pravastatin sodium are taken as the controlled-release parts at a tablet core part, wherein, the acipimox and the pravastatin sodium can be pressed into tablets by the form of a single tablet core or a dual-tablet core, and a compound osmotic pump preparation has the advantages of comprehensive action, low toxicity and side effects and convenient use.
US20130012512 P38 MAP kinase inhibitors There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.
CN103705521A Compound for treating cerebral infarction and application thereof The invention discloses a compound, a pharmaceutical composition thereof and new application, wherein the new application is the application for preparing medicaments for treating cerebral infarction. The compound can reach very substantial effect for treating cerebral infarction.
CN101897993A Method of soft tissue augmentation Particles according to the invention are made of a viscoelastic medium, are injectable gel particles, and have a size, when subjected to a physiological salt solution, in the range of from 1 to 5 mm. The particles are useful in a soft tissue augmentation implant. The implant comprises particles of a viscoelastic medium, wherein a major volume of the particles are injectable gel particles according to the invention. The implant is useful in a method of soft tissue augmentation in a mammal, including man, comprising subepidermal administration at a site in said mammal where soft tissue augmentation is desirable, of an implant according to the invention.
US20110230546 dsRNA COMPOSITIONS AND METHODS FOR TREATING HPV INFECTION The invention relates to a double-stranded ribonucleic acid (dsRNA) for treating human papilloma virus (HPV) infection. The dsRNA comprises an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of an HPV Target gene selected from among HPV E1, HPV E6 and the human E6AP gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by HPV infection and the expression of the E6AP gene using the pharmaceutical composition; and methods for inhibiting the expression of the HPV Target genes in a cell.
EP1813269A1 TRANSCRIPTIONAL FACTOR Nrf2 ACTIVATOR AND FOOD HAVING THE FUNCTION OF THE SAME IMPARTED THERETO A composition, an Nrf2 activating agent, and a food according to the present invention comprise isohumulones or isomerized hop extract as an active ingredient. They are useful in treating, preventing, or ameliorating a disease of condition which is treatable, preventable, or ameliorable by the activation of transcription factor Nrf2. More specifically, the composition, the Nrf2 activating agent and the food according to the present invention are useful in treating, preventing, ameliorating, or alleviating chronic diseases which are believed to be caused or exacerbated by cellular damages due to oxidative stress in the body or environmental substances (for example, arteriosclerosis, hypertension, diabetes, cerebral nerve degenerative diseases, skin diseases, eye diseases, asthma, and cancer) or delaying progress of these diseases, or in detoxificating xenobiotic substances.
US7947452 Oligonucleotides originating from sequences coding for the surface component of PTLV envelope proteins and their uses The invention relates to the use of oligonucleotides from the nucleotide sequences coding for the amino-terminal region of the surface component (SU) of envelope proteins of PTLV viruses in order to perform methods of detecting every PTLV strain or PTLV-related viruses, e.g. for the detection of novel PTLV variants or viruses comprising sequences related to PTLV SUs. The invention also relates to primer pairs which are used to perform said detection methods and the novel PTLV variants thus detected.
CN102241644A Alpha-azyl-3-aryl propionamido thiazole derivative, preparation method and purpose thereof The invention relates to the field of diabetes related medicament, and specifically relates to dipeptidyl peptidase-IV inhibitors, which have a general formula I and contain an alpha-azyl-3-aryl propionamido thiazole structure, and preparation method thereof, and also relates to pharmaceutical compositions containing the inhibitors and application thereof to preparation of diabetes medicaments, wherein groups are defined in specifications.
CN101780029A Antofloxacin oral preparation and application thereof The invention relates to an antofloxacin oral preparation which contains antofloxacin or salts and/or hydrate of antofloxacin, at least one filling agent and at least one binding agent, as well as 10-25 percent by weight of carboxymethyl starch. The antofloxacin oral preparation has enough hardness and better dissolution, and is mainly used for treating or preventing bacterial infection of people or animals.
CN102178740B Drug combination for treating burns and scalds, preparation method and application The invention discloses a drug combination for treating burns and scalds, a preparation method and application. The drug combination comprises mulberry bark, rapeseed oil, bee wax, bismuth subnitrate, prednisone and chloramphenicol. The treatment method for smearing the drug combination on burn and scald wounds is easy, and the mulberry bark and bee wax in the drug combination can spur the union of wounds and reduce formation of scars. The drug has a marked curative effect on III-degree burns and scalds.
WO2014011863A1 Method of treatment with 3-cyclopropylcarbonyl-3,6-diazabicyclo[3.1.1]heptane The present invention relates to 3-cyclopropylcarbonyl-3,6-diazabicyclo[3.1.1]heptane, its salt forms, pharmaceutical compositions, and methods of treatment thereof.
CA2542339A1 Combination of serotonin reuptake inhibitors and norepinephrine reuptake inhibitors This invention is directed in one embodiment to pharmaceutical compositions and methods for treating depression in a mammal. To a mammal in need of such treatment are administered: (i) at least one serotonin reuptake inhibitor or pharmaceutically acceptable salt thereof; and (ii) at least one norepinephrine reuptake inhibitor or pharmaceutically acceptable salt thereof, wherein the norepinephrine reuptake inhibitor is selected from the group consisting of Structure II, Structure III, and Structure IV as defined herein.
WO2011014883A3 Skin rejuvenation and wrinkle treatment by gingival fibroblast and its growth factor: activation of effect by hyluronic acid Disclosed herein is method a treating UVB-induced wrinkle or photo damaged skin by administering therapeutically effective amount of cultured GF-CM alone or in combination with Hyaluronic Acid subcutaneously via injection.
US20050043336 Quinazoline derivatives as antitumor agents The invention concerns quinazoline derivatives of Formula (I); wherein each of Q1, Q2, Z, R1, R2, R3, and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosin kinases.
US7615543 Complexes with C-reactive protein (CRP) molecules; rheumatoid arthritis, juvenile chronic (rheumatoid) arthritis, ankylosing spondylitis, psoriatic arthritis, systemic vasculitis, polymyalgia rheumatica, Reiter's disease, Crohn's disease and familial Mediterranean fever An agent for use in medicine, which agent comprises a plurality of ligands covalently co-linked so as to form a complex with a plurality of C-reactive protein (CRP) molecules in the presence thereof, wherein (i) at least two of the ligands are the same or different and are capable of being bound by ligand binding sites present on the CRP molecules; or (ii) at least one of the ligands is capable of being bound by a ligand binding site present on a CRP molecule, and at least one other of the ligands is capable of being bound by a ligand binding site present on a serum amyloid P component (SAP) molecule.
US20120029051 siRNA Targeting VEGFA and Methods for Treatment In Vivo Vascular endothelial growth factor A (VEGFA) is a chemical signal produced by cells that stimulates the growth of new blood vessels, and overexpression of VEGFA can lead to undesirable physiological conditions. Through the identification of new siRNA and modifications that improve the silencing ability of these siRNA in vivo, therapeutic compositions and methods have been invented to address the problems associated with this overexpression.
CN101219101A Fludarabine sustained-release implantation agent for treating solid tumors The invention relates to a solid tumors-curing fludarabine sustained-release implant, which is characterized in that the sustained-release implant contains effective anti-tumor dose of fludarabine, sustained-release auxiliary material and a certain amount of sustained-release regulator. Solid tumors consist of lung cancer, esophageal cancer, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic cancer, bladder cancer and colorectal cancer. The sustained-release auxiliary materials are mainly one or mixture of copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co-propyl phosphate). When the sustained-release auxiliary materials are degrading and absorbed, fludarabine is slowly released into tumor part, thus while reducing toxic reaction of the whole body, the sustained-release auxiliary materials can sustain concentration of effective drug at the tumor part. Placing the anti-tumor sustained-release implant at the tumor part can not only reduce toxic reaction of the whole body of fludarabine, but also improve drug concentration at the tumor part and enhance treatment effects of nonspecific treatments, such as chemotherapeutics, radiotherapy, etc.
CN102406622A Tolvaptan solid preparation The invention provides a tolvaptan solid preparation. The solid preparation is prepared from tolvaptan amorphous composition which is prepared by dissolving and drying tolvaptan and a carrier, as well as other pharmaceutically acceptable auxiliary materials, wherein the weight ratio of tolvaptan to the carrier is between 1:1.5 and 1:5. The preparation has the advantages of good solubility, good stability and high bioavailability.
US8507004 Use of MgO doped with a divalent or trivalent metal cation for removing arsenic from water Systems and methods for use of magnesium hydroxide, either directly or through one or more precursors, doped with a divalent or trivalent metal cation, for removing arsenic from drinking water, including water distribution systems. In one embodiment, magnesium hydroxide, Mg(OH)2 (a strong adsorbent for arsenic) doped with a divalent or trivalent metal cation is used to adsorb arsenic. The complex consisting of arsenic adsorbed on Mg(OH)2 doped with a divalent or trivalent metal cation is subsequently removed from the water by conventional means, including filtration, settling, skimming, vortexing, centrifugation, magnetic separation, or other well-known separation systems. In another embodiment, magnesium oxide, MgO, is employed, which reacts with water to form Mg(OH)2. The resulting Mg(OH)2 doped with a divalent or trivalent metal cation, then adsorbs arsenic, as set forth above. The method can also be used to treat human or animal poisoning with arsenic.
EP2590666A1 Topical application of erythropoietin for the treatment of eye disorders and injuries The invention relates to the use of erythropoietin (EPO), in particular EPO in a pharmaceutical preparation, for the treatment of traumatized or diseased eyes, in particular the case of endothelial dysfunction or dystrophies of the eye, preferably in connection with mechanical or pathological injuries of the cornea and conditions related thereto, as well as injuries following eye surgery.
WO2012125749A3 INFLAMMATION AND AUTOIMMUNE DISORDER TREATMENT USING RARα SELECTIVE AGONISTS The present specification provides compounds, compositions and methods using such compounds and compositions to treat an autoimmune disorder, inflammation and/or a transplant rejection.
CN101914080B Benzofuran-3-ketone substitute phenyl compound as well as preparation method and application The invention belongs to the technical field of medicaments, relating to benzofuran-3-ketone substitute phenyl compound as well as preparation method and application. The compound is prepared by preparing 5- methyl-2-(4- methoxy phenyl)-benzofuran by using 4-O-methyl iodide anisole and than reacting with 4-micristin. The compound prepared by the invention can be used for inhibiting the bioactivity of cancer cells and microbes.
US20080213351 Compositions and methods for dosing liposomes of certain sizes to treat or prevent disease The present invention relates to pharmaceutical compositions comprising liposomes and methods of using such liposomes to prevent, treat, or manage a variety of diseases and/or bodily conditions. The liposomes may comprise large unilamellar vesicles (LUVs) alone or in combination with multilamellar vesicles (MLVs), small unilamellar vesicles (SUVs), or other therapeutics. The invention relates to liposomes having certain diameters administered to patients using specific doses and/or dosing regimens.
WO2008097991A1 Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions This invention is directed to pyridopyrimidinone compounds of formula (I): wherein n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
WO2010029185A1 Oligosaccharide compounds for use in mobilising stem cells A compound of the following formula or a salt, solvate or formula (I) and a pharmaceutical composition containing said compound. It concerns also its use in the treatment of cancer and/or of pathological angiogenesis and/or in promoting the mobilisation of stem cells, in particular hematopoietic stem cells.
US20120142737 Pharmaceutical compositions of a non-enteric coated proton pump inhibitor with a carbonate salt and bicarbonate salt combination A method for treating gastric acid disorders with a non-enteric coated proton pump inhibitor in a pharmaceutically acceptable carrier including a bicarbonate salt of a Group IA metal and a carbonate salt of a Group IA metal; and a pharmaceutical composition of a non-enteric coated proton pump inhibitor in a pharmaceutically acceptable carrier including a bicarbonate salt of a Group IA metal and a carbonate salt of a Group IA metal are disclosed. A presently preferred proton pump inhibitor is lansoprazole, a presently preferred bicarbonate salt is sodium bicarbonate, and a presently preferred carbonate salt is sodium carbonate. The composition is a fast-acting formulation which reduces the undesirable belching associated with proton pump inhibitor formulations that contain high doses of sodium bicarbonate.
CN101433534A Use of resveratrol dimer for preparing medicament for reducing blood sugar The invention relates to the pharmacy field, in particular to medical application of resveratrol dimer. Pharmaceutical researches prove that the resveratrol dimer has obvious effect on inhibiting alpha-glucosaccharase, and can be used as hypoglycemic drugs, hypoglycemic health care foods or hypoglycemic foods.
WO2012161119A1 Novel spiropiperidine derivative and pharmaceutical product containing same Provided is a novel compound which has an effect of promoting insulin secretion from pancreatic β cells and is useful as a prophylactic and/or therapeutic agent for diseases associated with high blood sugar, such as diabetes. A compound represented by general formula (1), a salt thereof, or a solvate of the compound or the salt. (In the formula, ring A represents a C6-C10 aryl group or a five- to ten-membered heterocyclic group; Z represents O, N-R9, S(O)m, CH2 or C=O; each of R1, R2, R3 and R4 is independently absent or represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a hydroxyl group, a nitro group, a tetrazolyl group or the like; each of R5, R6 and R7 independently represents a hydrogen atom, a halogen atom, a cyano group or a carboxyl group; R8 represents a C1-6 alkyl group, a C6-10 aryl group or the like; each of R13 and R14 represents a hydrogen atom or a halogen atom; and R15 represents a hydrogen atom, a hydroxyl group or an oxo group.)
CN102488707A Preparation method and new application of polyinosinic preparation The invention relates to a preparation method and new application of a polyinosinic preparation. Kanamycin and calcium ions are added on the basis of polyinosinic, so that the stability of polyinosinic double-stranded ribonucleic acid (RNA) is enhanced. Animal experiment results show that a polyinosinic complex has the effect of inhibiting tumor growth.
US7517992 (-)-cis-1-(5-(4-fluorophenoxy)-pyridin-2-yl)-3-(4,7-difluoro-1,1a,2,7b-tetrahydro-cyclopropa[c]chromene-1-yl)-urea; improved resistance and pharmacokinetic profile; polymerase inhibitors; potent against virus comprising drug escape mutations A compound of the formula (Y): where; R1 is O, S; R2 is a nitrogen-containing heterocycle; R3 is H, C1-C3 alkyl; X is —(CR8R8′)n-D-(CR8R8′)m—; D is a bond, —NR9—, —O—, —S—, —S(═O)— or —S(═O)2—; n and m are independently 0, 1 or 2, R8 and R8′ are independently H, C1-C3 alkyl, haloC1-C3alkyl, hydroxy, or R8 and R8′ together with their adjacent C atom is —C(═O)—; R9 is independently H, C1-C3 alkyl; E is CH2—, —CHOH—, —C(═O)—, —NR9—, —O—, —S—, —S(═O)2—; n and m are independently 0, 1 or 2; p and q are independently 0, 1 or 2, where p+q≦2; R10 is an optionally substituted carbocycle or heterocycle; R11 is independently H, C1-C3 alkyl, halo substituted C1-C3alkyl, hydroxy; have utility as HIV antivirals.
CN102552266A Application of bisbenzylisoquinoline compound or pharmaceutically acceptable salt thereof in preparing medicine or healthcare product for improving sleep The invention discloses a new use of bisbenzylisoquinoline compound shown in formula (I) or pharmaceutically acceptable salt thereof except for tetrandrine and fangchinoline. The use is application of the bisbenzylisoquinoline compound shown in formula (I) or pharmaceutically acceptable salt thereof in preparing a medicine or healthcare product for treating insomnia and improving sleep. The bisbenzylisoquinoline compound shown in formula (I) or pharmaceutically acceptable salt thereof can be used as an effective component and made into any dosage form. The result of animal experiment indicates that: the bisbenzylisoquinoline compound shown in formula (I) or pharmaceutically acceptable salt thereof can obviously prolong the total sleep time of normal rats and mouse, including REM (rapid eye movement) sleep time and NREM (non-rapid eye movement) sleep time. The application disclosed by the invention is suitable for various types of insomnia or sleep disorders.
CN201510537U Rosuvastatin acid double-release capsule The utility model relates to a rosuvastatin acid double-release capsule agent which comprises a capsule outer casing and a medicament filled in a capsule inner casing, wherein the medicament is rosuvastatin rapid-release tablets and acid sustained-release tablets. The medicament has simple preparation technology, tablets do not need pressing twice, the hardness is proper, the tablet getting ratio is high, and the requirement to a pelleting machine is low. When the quality of the end product of the rosuvastatin acid double-release capsule agent is checked, the rosuvastatin acid double-release capsule agent has better accuracy compared with a capsule which is provided with double-layer tablets or is filled with small pills inside, and two components are not mutually interfered. More accurate relevant materials, contents, release rate and dissolution rate can be got.
CN101904863B Preparation process of medicinal composition compounded from astragaloside and astragalus polyose The invention discloses a preparation process of a medicinal composition compounded from astragaloside and astragalus polyose. The invention mainly relates to the preparation process of the medicinal composition compounded from the astragaloside and the astragalus polyose, in particular to a preparation process of a medicinal particularly injection standard composition, which adopts the combination of differential pressure type extraction, multi-stage membrane separation and concentration and column separation and refining, prepares high-purity astragaloside and neutral astragalus polyose at the same time by using the same batch of raw materials, and compounds the astragaloside and the astragalus polyose according to certain proportion.
US20050107458 used as diagnostic kits, bioassay and/or drugs for preventing cancers, Alzheimer's disease, amyotrophic lateral sclerosis, Parkinson's disease, stroke, ischaemia, Huntington's disease, epilepsy, multiple sclerosis, neuropathy, or injuries of the brain or spinal chord, or as tyrosine kinase inhibitors The present invention is directed to novel fused pyrrolocarbazoles and isoindolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.
CA2131662C Improved prodrugs for enzyme mediated activation Enzymatically cleavable prodrugs with reduced Michaelis-Menten constant (Km) are described.
US20080312254 Process for the Preparation of Ziprasidone The invention relates to processes for the preparation of substantially pure ziprasidone. The invention also relates to the preparation of acid addition salts of ziprasidone. More particularly, it relates to the preparation of substantially pure hydrochloride salt of ziprasidone. The invention also relates to pharmaceutical compositions that include the substantially pure ziprasidone or ziprasidone hydrochloride and use of said compositions for treating schizophrenia.
US20060281761 Osteoporosis; oral diseases; bone disorders; atherosclerosis; antiarthritic agents; autoimmune disease; cachexia Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, Alzheimer's disease, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
EP1776096A2 Crp lowering agent The present invention provides a novel drug which is useful as a preventive and/or therapeutic agent for various diseases involved in elevation of CRP level, in particular, inflammatory disease and cancer comprising a compound having inhibitory activity against squalene synthase or a salt thereof, or a prodrug thereof.
US20130065910 Oral meclizine aqueous formulations with taste flavoring agent An oral meclizine aqueous formulation is disclosed. The oral meclizine aqueous formulation comprises a solubizier for enhancing aqueous solubility of meclizine, and a taster flavoring agent selected from the group consisting of sugar, sucrose, sorbitol, sucralose, saccharin sodium, sodium cyclamate, aspartame, neotame, acesulfame potassium, stevioside, and their mixtures. Preferably the solubilizer is hydroxypropyl-β-cyclodextrin or polyethylene glycol 660 13-hydroxystearate. The oral meclizine aqueous formulation can provide a rapid onset of therapeutic effects of meclizine.
EP1994000A2 Water-soluble cc-1065 analogs and their conjugates This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
CN102145001B Stable aztreonam composition and preparation method thereof The invention belongs to the field of drug synthesis and preparations thereof, relates to a preparation method of an antibacterial drug, and particularly relates to a stable aztreonam composition and a preparation method thereof. The preparation method comprises the following steps: directly suspending aseptic beta-aztreonam in water, adding aseptic L-arginine to regulate the pH value for complete dissolution to obtain an aztreonam/arginine water solution, adding hydroxypropyl-beta-cyclodextrin (HP-beta-CD) into the water solution for clathration, subpackaging, and freeze-drying to obtain aztreonam for injection. The preparation method provided by the invention is simple and suitable for industrial production. After the aztreonam/arginine salt is clathrated by HP-beta-CD, the water solubility and stability of aztreonam are improved, the toxic and side effects of aztreonam are reduced, and the availability of aztreonam is improved.
WO2014054005A3 Nanosomal preparation of the complex formed by quercetin (or another flavonol, flavone or a derivative thereof) and 2-hydroxypropyl-β-cyclodextrin for intravenous use in cerebral pathological conditions The invention involves the preparation of cholesterol lecithin nanosomes, without propylene glycol, from the complex formed by quercetin (or another flavonol or flavone or a derivative thereof) and 2-hydroxypropyl-β-cyclodextrin, by means of a process that allows the safe, effective intravenous use thereof in the treatment of cerebral pathological conditions in adults and newborns. The preparation is safe, stabilizes the altered haemodynamic parameters in severe neonatal hypoxia in newborn pigs and is effective in protecting cerebral function in experimental Parkinson's disease models and in newborn pigs subject to hypoxia.
WO2007051119A1 Methods and compositions of parp inhibitors as potentiators in cancer therapy The present disclosure relates generally to a series of compounds which are derivatives of tricyclic compounds which inhibit poly (ADP-ribose) polymerase (PARP) and their use in the potentiation of cancer therapies. The disclosure relates more particularly to uses of azaphenanthridone compounds to chemosensitize cancers to the cytotoxic effects of chemopharmaceutical agents.
EP2174939A1 Pyranones useful as ATM inhibitors The application concerns a compound of formula Ia: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: Y is O; R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 6 ring atoms; R3 is wherein one of the phenyl rings in R3 bear a substituent selected from the group consisting of acylamido, sulfonamino, ether, ester, amido and acyl.
EP2340837A1 Combination treatment of cancer comprising EGFR/HER2 inhibitors The invention relates to a therapy of cancer comprising co-administration to a person in need of such treatment and/or co-treatment of a person in need of such treatment with effective amounts of: (1) a compound 1 of formula (I) wherein the groups Ra to Rd have the meanings given in the claims and specification; and (2) at least a further chemotherapeutic agent 2; optionally in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery, furthermore, the invention relates to corresponding medicaments and the preparation thereof.
CA2767296A1 Cyclic triazo sodium channel blockers The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula (I): in which z is a single bond or an optionally substituted linking group, R1 is a halo-alkyl group; and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system; or a salt thereof.
US20080027025 Protection From And Treatment Of Prion Protein Infection The disclosure for the first time provides an understanding of the mechanism of prion protein infection: prion proteins contain a cationic protein transduction domain (PTD) that interacts with the cell surface such that it induces macropinocytosis and enters the cytoplasm.
WO2012095505A1 Anticancer therapy with dual aurora kinase / mek inhibitors The invention describes anti-cancer therapies comprising using dual Aurora kinase / MEK inhibitors as descibed herein.
WO2008031835A2 Method of treating autoimmune diseases using vegf-pathway inhibitors The present invention relates to a method of treating a warm-blooded animal having an autoimmune disease, such as multiple sclerosis, peripheral neuritis, optical neuritis, amyotrophic lateral sclerosis or uveitis, comprising administering to said animal a therapeutically effective amount of a VEGF-pathway inhibitor, e.g. Bevacizumab, Sunitinib or Sorafenib, alone or in combination with further therapeutic measures; the use of a VEGF-pathway inhibitor for the preparation of a medicament for the treatment of an autoimmune disease; and to a commercial package comprising such a medicament together with instructions for its use in the treatment of an autoimmune disease.
US20100129464 Manufacturing method and apparatus for producing substances that include negative hydrogen ion A manufacturing method and apparatus produces various medium such as mineral substance, vitamin substance, or ceramic that include negative hydrogen icons for use by human beings and animals. In the manufacturing method, an optional mineral substance or vitamin substance as the medium in granular or powdered form is supplied to the inside of the container and filled with liquid hydrogen or hydrogen, gas. Then after leaving them in the container for a predetermined time, the medium is removed to be air dried, thereby producing the medium which is combined and included with negative hydrogen ion. Alternatively, high pressure, heat, or high voltage may be applied to the medium to contain the negative hydrogen ion in the medium.
US20100324072 Pyrrolopyridine derivatives and their use as bace inhibitors This invention relates to novel compounds having the structural formula I below: (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
WO2012070890A3 Pharmaceutical composition comprising extract of lonicera japonica for prevention and treatment of gastroesophageal reflux disease Disclosed is a composition for treating or preventing gastroesophageal reflux disease, which includes an organic solvent extract of Lonicerae Flos Thunberg. A fraction of the disclosed extract can be very effectively used for treating, preventing, or improving gastroesophageal reflux disease without side effects.
US8691981 Crystalline forms of (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide Crystalline forms of (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide of the formula (I) are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases.
WO2014138199A1 Pyrimidine compounds for the treatment of hepatitis c The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. I
US20080108683 4-phenylthiazole and 4-phenylimidizole derivatives and their use as medicaments for the treatment of neurodegenerative diseases, pain and epilepsy The invention relates to novel derivatives of 4-phenylthiazoles and 4-phenylimidizoles and the use thereof as medicaments. The invention especially relates to the following compounds: butyl-2-[4-(4-aminophenyl)-1H-imidizol-2-yl]ethyl-carbamate, and 4-[2-(1-aminocyclopentyl)-1,3-thiazol-4-yl]-2,6-di-tert-butylphenol, and the salts of the same.
WO2009071252A1 Nonsteroidal progesterone receptor modulators The present invention relates to nonsteroidal progesterone receptor modulators of the general formula (I), to the use of the progesterone receptor modulators for the preparation of pharmaceuticals, and to pharmaceutical compositions comprising said compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynecological diseases such as endometriosis, uterus leiomyomas, dysfunctional bleeding and dysmenorrhea and for the therapy and prophylaxis of hormone-dependent tumors and for use for female contraception and for hormone replacement therapy.
CN101016319A Benzoisoselenothiazolidone aminosugar derivative, preparing method and application therheof The invention discloses a making method and application of benzo isoselenazole aminosugar derivant with tumour resistance, which comprises the following steps: reacting 2-aminosurgar protected by hydroxy and amino acid protected by benzyl oxylcarbonyl group catalyzed by DCC; reducing reactant through hydrogen catalyzed by palladium carbon to remove benzyl oxylcarbonyl group; or reacting 2-aminosurgar protected by hydroxy and 2-cholbenzoyl chloride selenide catalyzed by trimethylamine directly.
CN1562080A Broad spectrum bacteriostat and sterilizing of silicate based angstrom silver ion nano porous composite mateiral A broad-spectrum antibacterial silicate-based angstrom Ag ion-nonoporous material able to kill more than 11 bacteria including ring worm, fungus, candida, blue mold, etc is prepared from the Ag ions and the silicate-base nanoporous material chosen from the molecular sieves of X-ray zeolite, A-type zeolite, Y-type zeolite, mordenite, etc.
EP1487836B1 Ethane-1,2-diamino-bis (2r)-2-bromo-3-phenylpropanoate|, method for production and use thereof The invention relates to ethane-1,2-diamino-bis[(2R)-2-bromo-3-phenylpropanoate], the production of ethane-1,2-diamino-bis[(2R)-2-bromo-3-phenylpropanoate] from (2R)-2-bromo-3-phenylpropionic acid and ethylendiamine in 2-propanol and the use of ethane-1,2-diamino-bis[(2R)-2-bromo-3-phenylpropanoate] for the production of ACE/NEP inhibitors.
CN101379046A Processes for taxane derivatives and intermediates useful therein The present invention provides a method for preparing taxane derivative and an intermediate product which can be used for the method.
US20120122816 Compositions and methods for organ preservation The invention relates to reducing, preventing or reversing organ damage, reducing and/or preventing stem cell damage and/or death, enhancing organ preservation and/or survival, or enhancing stem cell preservation and/or survival comprising administering a compound of formula A, a compound of any one of formulae 1-49 or I-III, a lipoxin compound, an oxylipin compound, or a combination of aspirin and an omega-3 fatty acid.
US20090169606 Low Flexural Strength Transdermal Tobacco Alkaloid Patch The invention relates to a tobacco alkaloid patch for transdermal administration of a tobacco alkaloid, said patch comprising an impermeable backing (17) and a membrane (14) which defines a reservoir (12) there between, said membrane (14) being permeable to and in contact with said tobacco alkaloid, said impermeable backing (17) and said membrane (14) being at least partly joined by a sealing (11), wherein said patch has a flexural strength of less than about 250 mN/mm. According to an advantageous embodiment of the invention, very high-dose nicotine patches may be obtained having acceptable membrane areas and featuring acceptable user comfort.
CN102406607B Tiopronin liposome injection The invention discloses a tiopronin liposome injection and a preparation method thereof. The tiopronin liposome injection is prepared from tiopronin, cholesterol, distearoyl phosphatidyl choline, twain 65, PEG (polyethylene glycol) 1000, trehalose and glutathione according to a specific weight ratio and has good stability; liposome does not crack because of fusion, ice crystal and the like and can keep excellent entrapment rate after the tiopronin liposome injection is stored for a long term. Through the invention, the stability of tiopronin is improved, the quality of the tiopronin liposome injection product is improved, toxic and side effects of the tiopronin liposome injection are reduced, retention time of medicine is increased in systemic circulation, the bioavailability of medicine is improved, and treatment effect is enhanced greatly.
US20090088408 Pharmaceutical compositions on anticholinergics, corticosteroids and betamimetics The present invention relates to novel pharmaceutical compositions based on anticholinergics, corticosteroids and betamimetics, processes for preparing them and their use in the treatment of respiratory diseases.
CN103156813A Fosaprepitant dimeglumine injection composition and preparation method thereof The invention relates to the field of medicament preparation, and particularly relates to a fosaprepitant dimeglumine injection composition and a preparation method thereof. The pharmaceutical active ingredients of the fosaprepitant dimeglumine injection composition include the following components in parts by weight: 180-250 parts of fosaprepitant dimeglumine, 12.0-20.0 parts of disodium edetate, 50.0-80.0 parts of polysorbate-80, 250-400 parts of lactose and 2000-3000 parts of water for injection. The preparation method comprises the following steps: dissolving, preparing, adsorbing, pre-freezing, performing sublimation drying and mounting an injection piston. The fosaprepitant dimeglumine injection composition provided by the invention is prepared from the low low-cost auxiliary materials according to a self-developed formula, has the same medicament effect in comparison with the existing fosaprepitant medicament available in America, is low in medicament cost and has no side effect basically; and the lactose used as excipient resists infection and is easy to absorb, so that favorable pharmaceutical effect can be achieved, and crushing of the medicament during storage can be avoided.
WO2010104056A1 Lifespan-extending agent Disclosed is a lifespan-extending agent which can inhibit senility caused by aging in individuals, is effective on the maintenance of homeostasis in living bodies, and can extend a lifespan in a safe manner even when ingested continuously for a long period. Specifically disclosed is a lifespan-extending agent, an anti-aging agent, or a Klotho protein expression enhancer comprising activated charcoal as an active ingredient. The lifespan-extending agent, the anti-aging agent or the Klotho protein expression enhancer has substantially no adverse side effect and can extend a lifespan when administered in the form of an oral preparation.
EP1517891A1 Diphenyl azetidinones substituted by acidic groups, method for their production, medicaments containing said compounds and use thereof The invention relates to compounds of formula (I), in which R1, R2, R3, R4, R5 and R6 are defined as cited, in addition to their physiologically compatible salts. The compounds are suitable for use e.g. as hypolipidaemics.
CN101331133A Sulphonamidoaniline derivatives being Janus kinases inhibitors The invention relates to sulphonamidoanilines of formula (I) wherein A is N or CH, W, X, Y and Z are N or CH under the proviso that at least one of the three symbols W, X and Y represent CH, R<1> represents NR4R5 or OR4, wherein R4 represents optionally substituted alkyl, optionally substituted cycloalkyl optionally comprising one or two nitrogen or oxygen atoms, or substituted aryl, and R5 represents hydrogen or unsubstituted or substituted alkyl, or R4 and R5 together with the nitrogen to which they are attached represent an optionally substituted five- or six-membered nitrogen containing monocyclic ring, an optionally substituted nitrogen containing fully saturated bicyclic ring, or an spirocyclic fully saturated ring system containing one or two nitrogen atoms, R<2> is hydrogen, lower alkenyl or alkyl, R<3> is alkyl which is unsubstituted or mono-, di- or trisubstituted by halogen; alkenyl or aryl, and their salts; processes for their preparation, their application in the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment of diseases, a method for the treatment of such a disease and the use of such a compound - alone or in combination with one or more other pharmaceutically active compounds - for the manufacture of a pharmaceutical preparation for the treatment of a proliferative disease.
CN103230413A Compound omeprazole preparation The invention provides a compound omeprazole preparation. According to the invention, the preparation is composed of micronized proton pump inhibitor omeprazole, an anti-acid agent sodium bicarbonate, and common pharmaceutically acceptable auxiliary materials. According to the invention, micronization process conditions are optimized, and micronization vibration frequency is adjusted, such that medicine particle size rang is effectively controlled. With the method, medicine dissolution rate and bioavailability are improved, and process controllability and stability are enhanced. According to the invention, omeprazole medicine is crushed with an independent micronization method or by combined micronization with the anti-acid agent and/or a filling agent. Particle size distribution is controlled within the range of d90 (20mum), d50 (4mum), and d10 (2mum). Compared with reference preparations in the market, the process stability is high, and dissolution effect is good.
CN103181917A Potassium aspartate pharmaceutical composition and preparation method thereof The invention relates to a pharmaceutical composition, and particularly relates to a pharmaceutical composition comprising potassium aspartate, aerosol, and medically acceptable carriers, a preparation method and applications thereof.
CN101450914B Novel benzoic acid derivatives The invention belongs to the technical field of medicine, in particular to novel benzoic acid derivatives shown in the general formula (I), pharmaceutically acceptable salts or stereoisomers thereof, wherein R<1>, R<2>, R<3>, R<4>, R<5>, R<6> and Ar are defined as the description. The invention also relates to a method for preparing the compounds, medical compositions containing the compounds, and application of the compounds in preparing medicines for treating and/or preventing infectious disease.
US7579344 Pyrimidine derivatives possessing cell-cycle inhibitors activity Compounds of the formula (I), and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti cell proliferation) effect in a warm blooded animal, such as man.
US7479564 e.g. 6-ethyl-5-(4-{2-[({[(4-methylphenyl)sulfonyl]amino}carbonyl)amino]ethyl}phenyl)-5H-[1,3]dioxolo[4,5-f]benzimidazole; prostaglandin E2 receptor antagonists; arthritis, hyperalgesia, uterine contraction, digestive peristalsis, awakeness, blood pressure, platelet function, bone metabolism, angiogenesis This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl ; R5 is H, C1-4 alkyl, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamadin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
WO2013116291A1 Imidazo [4, 5 - b] pyridine derivatives as alk and jak modulators for the treatment of proliferative disorders This application relates to compounds of the Formula I as defined herein, and/or salts thereof. This application further relates to compositions and methods of using these compounds and/or salts thereof. The compounds of Formula I are useful as ALK and JAK modulators for the treatment of proliferative disorders.
US6960592 erectile dysfunction; halosulfonation of 2-ethoxy benzoic acid, sulfonamidation, haloacylation, deacylation and amidation, cyclization; phosphodiesterase inhibitor; side-effect reduction; long lasting The present invention relates to new 1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one compounds of formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, useful for treatment of impotence diseases: wherein R1 and R2 may be the same or different and independently be C1-6 alkyl. The present invention also provides a method of preparing the compounds of formula (I).
CN103156860A Olanzapine composition and preparation method thereof The invention provides a composition comprising olanzapine crystalline particles with an average particle size equal to or smaller than 30 [mu]m and a pharmaceutically acceptable carrier. The olanzapine crystalline particles with the average particle size equal to or smaller than 30 [mu]m are basically bioequivalent. The composition can be used for treating mental diseases such as schizophrenia.
US20120101163 Composition for inhibiting cancer metastasis The invention provides a composition for inhibiting cancer metastasis, including: an effective amount of an amino acid hydroxamic acid derivative having a formula as shown as formula (I), formula (II) or formula (III): and a pharmaceutically acceptable carrier or salt, wherein the amino acid hydroxamic acid derivative has an effect for inhibiting cancer metastasis.
CA2360590C Solution-based transdermal drug delivery system An efficient transdermal delivery system for delivering an active ingredient to the blood supply of a living body, comprising a vasodilator, an active ingredient, and a permeation enhancer for the active ingredient. The components of this mixture are combined in a manner that dissolves them into solution, eliminating the need for a polymeric binding agent and thus diminishing the total molecular weight of the mixture and increasing the penetration and delivery efficiency of the active drug molecules.
WO2013007792A1 Novel th2 polarizing compounds The present invention relates to a pharmaceutical composition, particularly to a pharmaceutical composition for use in the treatment and/or prevention of immune-mediated diseases which are characterized by a Th1 environment such as autoimmune diseases, wherein said pharmaceutical composition comprises a compound of formula (I) as defined herein. The present invention also relates to the use of a compound according to formula (I) as defined herein for activating the production of at least one Th2 polarizing cytokine in NKT cells.
WO2010080357A1 Serotonin 5-ht2b receptor inhibitors Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds.
CN103182063A Chinese patented drug pill for treating cancer The invention discloses a Chinese patented drug pill for treating a cancer, which can quickly treat and cure various pains due to the cancer with curative effect, eliminate active malignant tumors, inhibit generation of new malignant tumors, comprehensively repair and heal surgical treatment caused incision and diseased tissues and organs, suppress reaction and formation of cancer cells, and effectively decompose and make the cancer cells apoptotic. In recent more than half a century, people have paid a lot to treat the cancer, but at present the cure ratio is less than 1%, which is the result of failed Western traditional researches, and indicates that the western medicines cannot conquer the cancer cells. Drug preparation inland does not cause technical cost or take risks, and furthermore the approval of drugs is also easy. The present invention is based on the literature 'Green purification therapy treatment of the cancer by breaking through cancer theoretical understanding of world science' to treat the cancer. The early promotion of the drug pill is also full of practicable public significance.
CA2282183C Oxy substituted 4-carboxyamino-2-methyl-1,2,3,4-tetrahydroquinolines Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
CN1965650A Multiple metal ion chelated green antibacterial agent of chitosan The invention relates to an environment-friend antibacterial agent, wherein the inventive antibacterial agent can improve immunity, accelerate cell growth and repair. The invention is characterized in that: its corn is crust element and combined Ag, Zn, Cu metal ion which is removed from acetyl. The solution of said antibacterial agent is in yellow, green, blue and transition color, or transparent achromatic color. And the powder agent can be micro crystal, nanometer powder, or film agent.
WO2008021378A1 Use of adsborbent carbon microspheres to treat intestinal bacterial infections Disclosed herein is the use of adsorbent carbon microspheres for the treatment of intestinal bacterial infections. The infections include infection with Escherichia coli, Shigella dysenteriae, Vibrio cholerae, and Clostridium difficile. The adsorbent carbon microspheres serve to adsorb or bind toxins produced by the bacteria.
US20130045957 Prevention of and Recovery from Drug-Induced Ototoxicity Provided herein are methods for preventing and/or reducing the severity of drug induced ototoxicity. Provided herein are methods for recovery from hearing loss due to drug-induced ototoxicity.
EP2207777A2 Polymorphs of dasatinib and process for preparation thereof Provided is dasatinib, solvates thereof and their crystalline forms, methods for their preparation, and pharmaceutical compositions thereof. Formula (I).
US20090143427 4-Oxoquinoline derivatives This invention relates to novel compounds that are 4-oxoquinoline derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 4-oxoquinoline derivatives that are derivatives of elvitegravir. This invention also provides pyrogen-free compositions comprising one or more compounds of this invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an HIV integrase inhibitor, such as elvitegravir.
WO2006106839A1 METHOD FOR SCREENING AUXILIARY AGENT CAPABLE OF PROMOTING THE INDUCTION OF INTERFERON-α AND/OR -β (IFN-α/β) EXPRESSION Disclosed is a method for screening an auxiliary agent capable of promoting the induction of the expression of interferon-α and/or -β (IFN-α/β). The method comprises the steps of: a) in a cell/nucleic acid adjuvant system in which the expression of IFN-α/β is not induced in the absence of the auxiliary agent, incubating the cell together with the nucleic acid adjuvant in the presence or absence of a candidate compound for the auxiliary agent; b-1) confirming the presence of the intracellular movement of the nucleic acid adjuvant into an endosome vesicle by the action of the candidate compound or b-2) confirming the presence of the induction of the expression of IFN-α/β by the action of the candidate compound; and c) regarding the compound as an effective auxiliary agent when the movement of the nucleic acid adjuvant into an endosome vesicle or the induction of the expression of IFN-α/β is recognized in step b-1) or b-2).
US20100173928 Phosphorylation and regulation of AKT/PKB by the rictor-mTOR complex In certain aspects, the invention relates to methods for identifying compounds which modulate Akt activity mediated by the rictor-mTOR complex and methods for treating or preventing a disorder that is associated with aberrant Akt activity.
CN103239432A Compound ambroxol hydrochloride composition granule and preparation method thereof The invention relates to the field of pharmacy and discloses a compound ambroxol hydrochloride composition granule. 1000 granules of drugs are prepared from the following active ingredients: 7.0-8.0g of ambroxol hydrochloride, 1.5-2.5g of salbutamol sulfate, 900-1000g of cane sugar and defined amount of purified water. The compound preparation formed by ambroxol hydrochloride and salbutamol has the beneficial effects that through synergistic action of the two drugs, the functions of expelling phlegm to arrest coughing and resisting asthma can be simultaneously achieved, the cough symptom can be quickly relieved, and sputum removal can be promoted; secretions and bronchospasm accompanying asthma and acute and chronic bronchitis can be better controlled by using the two drugs jointly; and through drug combination, not only are the lung functions improved but also the number of asymptomatic days of patients is increased, and the life quality of the patients is improved. The invention also discloses a preparation method of the compound ambroxol hydrochloride composition granule. The preparation method is simple in process steps, is easy in process parameter control and is suitable for large scale production.
CN1568952A Peroral blood sugar reducing compound pharmaceutical preparation The invention discloses a blood sugar reducing compound pharmaceutical preparation, which comprises biguanides medicament (metformin hydrochloride) and third generation sulfonylureas medicament (glimepiride) and findings. The medicament can be prepared into the dosage forms of hard capsule, stomach dissolving tablet, and slow release tablet.
US20080132554 Crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol The present invention is directed to an anhydrate crystal form (Form D) of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol, an estrogenic receptor modulator useful in the treatment of, for example, diseases related to abnormal levels of estrogen.
WO2006054536A1 Therapeutic agent for urolithiasis A ureteral peristalsis movement accelerator which contains a compound represented by the general formula (1) [wherein R represents optionally hydroxylated alkyl] or a pharmaceutically acceptable salt thereof as an active ingredient. In animals including human beings, the accelerator can increase the amplitude or frequency of peristalsis movements of the ureter. Because of this effect, the accelerator is useful for the treatment or prevention of urolithiasis.
WO2009100949A1 Zwitterionic guanidinium compounds as selective antimicrobial active ingredients The invention relates to a use of compounds corresponding to formula I and/or a physiological salt thereof and/or stereoisomer forms thereof, as selective antimicrobial active ingredients, wherein R1-R5 can be a hydrogen atom or a (C1-C3)-alkyl residue, R6 -(CH)2-COO- with n=0-4, -(CH2)n-SO3- with n=0-4, or an amino acid substituent, such that the amino group of the amino acid part can be a guanidinium derivative corresponding to formula I and/or R1 and R6 can form a structural element of the formula II, wherein R9 can be a hydrogen atom, a (C1-C3)-alkyl residue, -(CH2)n-COO- with n=0-4, or -(CH2)n-SO3- with n=0-4, R7 and R8, independently of one another, can be a hydrogen atom, a (C1-C3)-alkyl residue, a hydroxyl group, -(CH2)n-COO- with n=0-4, or -(CH2)n-SO3- with n=0-4 and X can be 1, 2, or 3. 2. Use according to claim 1, characterized in that the compound according to formula I is creatine. 3. Use according to claim 1, characterized in that the compound of formula I is the cyclic guanidinium derivative of the compatible solute ectoin or S,S-ß-hydroxyectoin. 4. Use according to one of claims 1 through 3 in the food industry and in domestic hygiene.
US20110165098 Methods to prevent cytotoxicity using n-acetyl-cysteine Compositions and methods to inhibit adverse physiological effects caused by resin-based and resin-containing materials are disclosed. More specifically, the use of N-acetyl-cysteine (NAC) to inhibit hydroxyethyl methacrylate (HEMA)-mediated cell death and cytotoxicity.
WO2008053764A1 Anti-prion active compound, anti-prion active agent, and method for inhibition of the production of abnormal prion protein [PROBLEMS] To provide an anti-prion active compound having an excellent effect of preventing the increase in the level of an abnormal prion protein, and also provide an anti-prion active agent and a method for inhibiting the production of an abnormal prion protein, both utilizing the anti-prion active compound. [MEANS FOR SOLVING PROBLEMS] The anti-prion active compound is a pyrazolone derivative represented by the general formula (1). (1) wherein R1 represents an aryl group which may have a substituent or an alkyl group (including a cycloalkyl group) which may have a substituent; R2 represents a hydrogen atom, an aryl group which may have a substituent, a nitrogenated heterocyclic functional group which may have a substituent, an alkyl group (including a cycloalkyl group) which may have a substituent or an acyl group ; and R3 represents an aryl group which may have a substituent, an alkyl group (including a cycloalkyl group) which may have a substituent, RCONH-, RNHCO-, ROCONH- or RNHCONH- [wherein R represents an aryl group or an alkyl group (including a cycloalkyl group)].
WO2008147956A2 Toll-like receptor 3 modulators and uses thereof Modulators of TLR3 activity and their use are disclosed.
CN1657618B Hepatic correlative oncogene inhibitory and use A cancer-suppressing gene LFIRE-1 associated with liver, which has the specific expression, low expression, or no expression in human liver and the suppressing action to the growth of liver cancer cells, the preparing process of human LFIRE-1 polynucleotide and polypeptide, their application in diagnosing and treating liver cancer, and the relative test reagent kit and medicines are disclosed.
US7829672 Modulation of sodium channels in dorsal root ganglia A novel tetrodotoxin resistant sodium channel is described, along with isolated nucleotides that encode this receptor. Methods for identifying agents that modulate the Na+ current through the receptor are provided, as well as related therapeutic and diagnostic methods.
CN102372703A Indole benzothiazole derivative and pharmaceutical use thereof The invention, belonging to the field of biological pharmacy, relates to an indole benzothiazole derivative and an application of the derivative for preparing inhibitors of 5-HT receptor, especially an application in the field of medicines of nerve system diseases related to the 5-HT receptor. The test of bioactivity shows the indole benzothiazole derivative has inhibiting effect on the 5-HT receptor related to the pathological mechanism of nerve system diseases. The derivative can be used as a medical precursor for synthesizing the inhibitor of the 5-HT receptor, further can be used for preparing medicines for schizophrenia, parkinsonism and other nerve system diseases caused by disfunction of the 5-HT system.
CN102000047B Antrodia camphorata cyclonene compound for restraining growth of bone cancer cells The invention relates to a novel application of a compound. In the invention, 4-hydroxy-2,3-dimethoxy-6-methyl-5(3,7,11-trimethyl-2,6,10- cyclododecatriene)-2- cyclonene(4-hydroxy-2,3-dimethoxy-6-mehty-5(3,7,11-trimethyl-dodeca-2,6,10-trienyl)-cyclohex-2-enone) is separated and purified from an antrodia camphorate extract. The cyclonene compound can be applied to restricting the growth of a bone cancer cell and the medical composition for restricting the growth of bone cancer cells.
CN101190933A 6-O-methylerythromycin A crystal form III The invention relates to a novel compound of 6-O-Methylerythromycin A crystal form III and the preparation method thereof, comprising the medical components of the compound and the usage method of the compound, which is taken as a healer.
CN103127340A Ointment for curing scald and burn An ointment for curing a scald and a burn is composed of bulk pharmaceutical chemicals including: 15 to 26 parts of momordica cochinchinensis, 17 to 28 parts of fructus gleditsiae, 16 to 25 parts of ground beeltle, 18 to 25 parts of immature bitter orange, 13 to 19 parts of dragon blood, 5 to 15 parts of calomel, 3 to 10 parts of borneol and 1 to 8 parts of musk. The ointment for curing scald and burn has the advantages of being free of an injection and medicine under general condition, not weaving skin, being antisepsis and anti-inflammation, rapidly removing a necrotic tissue and promoting tissue regeneration, promoting growth of muscles and bones, being free of anaphylactic reaction, being free of leaving sequelae such as scars and spots and being easy to operate, less in medicine expense and short in course of treatment. Generally, moderate and minor wounds can be cured in one week, and severe wounds can be cured in about half a month. The ointment for curing the scald and the burn is good in effect. According to statistics, 363 cases of patients with minor, moderate and severe wounds caused by scalding, burning and frying are cured from 1980 to 2000, wherein the 363 cases include 68 cases of minor wounds, 235 cases of moderate wounds and 60 cases of severe wounds, all the patients are cured, and the cure rate reaches 100%.
WO2009037302A1 5-substituted-1, 4-benz0diazepines as phosphodiesterase inhibitors Novel 7, 8 dialkoxy-5 - (amino alkyl phenyl) - 1, 4 -benzodiazepines of formula I with said amino being substituted or forming a nitrogen containing heterocyclic alkyl ring, which 1, 4- benzodiazepines are inhibitors of phosphordiesteraste type IV (PDE-4) making then active as anti- inflammatory agents.
US20100160439 Dermatological compositions comprising at least one retinoid compound, an anti-irritant compound and benzoyl peroxide Dermatological compositions contain, formulated into a physiologically acceptable medium, at least one retinoid compound selected from among all-trans retinoic acid, isotretinoin, motretinide, and naphthoic acid compounds of formula (I), and salts and esters thereof: wherein R is a hydrogen atom, a hydroxyl radical, a branched or unbranched alkyl radical having from 1 to 4 carbon atoms, an alkoxy radical having from 1 to 10 carbon atoms, or a cycloaliphatic radical which is substituted or unsubstituted, and benzoyl peroxide, and also at least one anti-irritant compound selected from among 18β-glycyrrhetinic acid, and its salts and derivatives thereof.
WO2010112116A1 Heterocyclic compounds as autotaxin inhibitors The invention relates to compounds of the formula I, where Het, R, X, Y, R1, and p have the meanings given in Claim 1, wherein said compounds are autotaxin inhibitors and can be used for treating tumors.
WO2006125800A1 17β-HSD1 AND STS INHIBITORS The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration.
US20130267601 Method for prevention of alzheimer's disease A method for prevention of Alzheimer's Disease (AD) is presented. The principal cause of AD is a deficiency at the cellular level of the human brain, of the effects of the active form of thyroid hormone, tri-iodothyronine (T3). Lifelong T3 replacement, beginning in early to mid life and, in some cases later, overcomes these blocks to T3 production and actions and prevents AD in a majority of the sub-types of AD.
CN101406560A Stype for treating ankylosing spondylitis and preparation method thereof The invention discloses a stype for treating ankylosing spondylitis. The stype for treating ankylosing spondylitis is prepared from pure natural plants and animals taken as raw materials according to a certain process; the stype has wide material source, low cost and simple preparation process; and the stype has wide range, high cure rate, low treatment expense and no recrudescence after healing for treating ankylosing spondylitis.
WO2012133733A1 Cancer cell proliferation inhibitor A cancer cell proliferation inhibitor which comprises, as the active ingredient, a triterpene derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof. In general formula (I): R1 represents a carboxyl group or a hydroxymethyl group; and R2 represents a benzyl group optionally substituted by a hydroxymethyl group, a C1-6 alkyl group, a C2-6 alkenyl group or a C2-6 alkynyl group.
WO2008060112A1 Composition comprising araliae cordatae radix extract or compounds isolated from the same for preventing or treating periodontitis The present invention relates to a composition comprising an Araliae Cordatae Radix extract or compounds isolated from the same for preventing or treating periodontitis. The Araliae Cordatae Radix extract or compounds isolated from the extract according to the present invention has/have excellent antimicrobial and bactericidal activities against Porphyromonas endodontalis, Porphyromonas gingivalis and Prevotella intermedia, which are periodontal pathogens, thereby being used to prevent or treat periodontitis.
US20110009419 Enantiomers of 2'-Fluoralkyl-6-nitroquipazine as Serotonin Transporter Positron Emission Tomography Imaging Agents and Antidepressant Therapeutics Racemic mixtures and individual enantiomers of fluorine-18 or carbon-11 radiolabelled 2′-alkyl-6-nitroquipazine ligands are serotonin transporter (SERT) tracers for positron emission tomography (PET) imaging. The non-radioactive ligand forms possess therapeutic antidepressant in vitro and in vivo pharmacological binding profiles in rodent brain and cells expressing human serotonin transporter (hSERT). Twelve 2′-alkyl-6-nitroquipazine ligands potently bind in sub-nanomolar concentrations to the pre-synaptic SERT binding site where established antidepressant drugs bind and inhibit the re-uptake of the neurotransmitter serotonin (5-HT). In vivo tracer studies in rats as well as monkey PET scan trial have demonstrated the fluorine-18 and carbon-11 positron radionuclide labeled tracers perform as quantitative tracers of specific binding the SERT protein in live brain.
CN101301470A Anticancer composition containing neovascularization inhibitor and bortezomib The invention provides a sustained-release injection which is an anti-tumor composite containing agiogenesis inhibitors and bortezomib. The sustained-release injection comprises a sustained-release microsphere and a solution medium, wherein the sustained-release microsphere comprises effective anti-tumor ingredient and sustained-release excipient, the solution medium is a common solution medium or a special solution medium containing a suspending drug. The suspending drug has the viscosity between 100cp and 3000cp (under twenty centi degrees to thirty centi degrees) and is selected from sodium carboxymethylcellulose and others; the effective anti-tumor ingredient comprises the agiogenesis inhibitors and/or the combination thereof; the sustained-release excipient is selected from polyphosphonate copolymer like p(LAEG-EOP)or p(DAPG-EOP), PLA, polyphosphonate with PLA, polifeprosan, copolymer of dual fatty acid and sebacic acid, the polymer or blending polymer of ( erucic acid dipolymer-sebacic acid) or poly(boletic acid-sebacic acid); the anti-tumor composite can also be prepared to be a sustained-release implant which can maintain the effective concentration of drug over forty days for intratumor or tumor circumference injection or placement, can also reduce general reaction obviously and enhance the treatment effect of non-operative therapeutics such as chemotherapy and radiotherapy.
WO2007092721A8 Vitamin d analog: rak, methods and uses thereof Compounds of formula (IA) or (IB) are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms; straight or branched chain alkenyl groups having from 2 to 8 carbon atoms; straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms; straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
US20090035389 Targeted protein cages The present invention provides targeted protein cages for the specific delivery of a variety of agents to cells and tissues and methods of use. The targeted protein cages have exterior targeting moieties and therapeutic or imaging agents which are encapsulated within the protein cages or are located on the exterior surfaces of the protein cages.
US20120231073 Dexlansoprazole compositions Premixes of dexlansoprazole with pharmaceutical excipients, processes for preparing premixes, pharmaceutical formulations containing the premixes, and their use in treatment of erosive esophagitis and heartburn associated with non-erosive gastroesophageal reflux disease.
DE102010055585A1 Nanoparticles useful for treating rheumatic diseases comprises amorphous ferrosilicon exhibiting magnetizable properties Nanoparticles comprises amorphous ferrosilicon exhibiting magnetizable properties. - ACTIVITY : Antirheumatic. No biological data given. - MECHANISM OF ACTION : None given.
EP2099803A1 Heterobicyclic matrix metalloprotease inhibitors The present invention relates generally to amide containing heterobicyclic containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors.
US20080064679 Water Soluble Cannabinoids Water-soluble cannabinoid compounds that are agonists of CB1 and CB2 cannabinoid receptors are provided. The compounds are made water-soluble by derivatization of the alkyl side chain and/or the phenolic hydroxyl group of tetrahydrocannabinol. The water-soluble cannabinoids are useful for the treatment of appetite loss, pain, multiple sclerosis, nausea and vomiting, and epilepsy.
US20100203100 Antimicrobial accessory for an implantable medical device An antimicrobial accessory may include a pressure sensitive adhesive and an antimicrobial mixed in the pressure sensitive adhesive. In some examples, an antimicrobial accessory may include at least one first domain comprising a pressure sensitive adhesive and a first antimicrobial and at least one second domain including a second polymer and a second antimicrobial. The antimicrobial accessory may be configured to be attached to a housing of an implantable medical device (IMD).
US20110065756 Methods and compositions for treatment of obesity-related diseases The invention relates to methods, compositions, and kits for combination therapy of diabetes and diabetes-related diseases and conditions (e.g., obesity). The invention finds use in patients suffering from or at risk for diabetes or diabetes-related conditions generally, and in patients also suffering from or at risk for fluid retention (e.g., edema, congestive heart failure) and/or in need of synergistic anti-inflammatory, anti-hypertensive, and anti-diabetic effect.
WO2011049539A1 Compositions comprising a corticosteroid, a beta2 agonist as well as cromoglicic acid or ndeocromil The present invention relates to a pharmaceutical composition for use in the treatment of respiratory diseases, characterized in that said composition comprises a pharmaceutically effective amount of cromoglicic acid and/or nedocromil salts besides β2-agonists and corticosteroid drugs.
WO2012090676A1 Novel medicinal composition and utilization of same The purpose of the present invention is to safely treat or prevent, without difficulties in drug selection or dose design and without side effects, developmental disorder, schizophrenia, mood disorder, eating disorder, a mental disease following cerebrovascular disorder or a mental disease following head trauma, and to potentiate the effect of a therapeutic for cognitive impairment or an antidepressant. A medicinal composition according to the present invention, which comprises, as the active ingredient, at least one compound selected from the group consisting of ferulic acid, an ester thereof, a pharmacologically acceptable salt of the same and a pharmacologically acceptable solvate of the same, can be used, either alone or in combination with an active ingredient of a therapeutic for the aforesaid diseases or disorders, for treating the diseases or disorders.
WO2005030953A1 Tetrahydrofolate synthase gene It is intended to find a novel tetrahydrofolate synthase gene and a protein encoded by this gene and thus provide a method of identifying a compound inhibiting the cell growth promoting activity of the protein. It is also intended to provide a method of judging colon cancer, a method of preventing the same and a method of treating the same. Namely, a DNA containing the base sequence consisting of the 94th- to 2934th-bases in the base sequence represented by SEQ ID NO:1 in Sequence Listing; a polynucleotide hybridizable specifically with this DNA;a protein encoded by this DNA; a recombinant vector containing this DNA; a transformant containing this recombinant vector; an antibody against the above protein; a process for producing the protein; a method of identifying a compound inhibiting the cell growth promoting activity of the protein; a method of judging colon cancer characterized by comprising measuring the expression amount of the above DNA; a kit for judging colon cancer; and a preventive and/or a remedy for colon cancer.
CN103735754A Preparation method of lipid-lowering medicine The invention discloses a preparation method of a lipid-lowering medicine. The preparation method comprises the following steps: respectively grinding 10g of nitroglycerin tablets, 8g of seman sinapis albae, 10g of rhizoma alismatis and 16g of liquoric root, mixing uniformly, and sieving with a 180-mesh sieve to obtain the lipid lowering medicine. In the invention, the lipid lowering drug is prepared by combining the Chinese and western medicines and has low price and mild characters; the preparation is stable, safe and reliable without adverse reaction, does not cause any harm to the hepatic and renal function, and has remarkable anti-allergic and detoxifying effects.
US20130052153 Method of preparing hydrogel structure A method of preparing hydrogel structure, wherein the hydrogel structure comprises: (a) a one way penetrating polyurethane film layer, (b) a hydrophobic pressure sensitive adhesive layer, (c) a multi-directional elastic meltblown nonwoven, (d) an interpenetrating polymer network, and (e) a hydrophilic hydrogel; and the method comprises: (i) coating the hydrogel in a form of solution on the meltblown non-woven to form a product 1, (ii) UV curing the product 1 in step (i), forming a composite comprising a hydrogel layer on the top, an interpenetrating polymer network in the middle, and a meltblown non-woven layer on the bottom, wherein the interpenetrating polymer network is a mixture of the hydrogel and the meltblown non-woven, (iii) providing polyurethane film layer coated with pressure sensitive adhesive layer, and (iv) laminating part of exposed fibers of meltblown non-woven with the pressure sensitive adhesive layer, forming a hydrogel structure.
CN102600458A Compound preparation of glucosamine chondroitin and production method of compound preparation The invention discloses a compound preparation of glucosamine chondroitin. The compound preparation comprises the following main components of: glucosamine salts and chondroitin sulfate as main active components, one or several of dimethyl sulfone and collagen as auxiliary components and an accessory. Mixed granules produced by the compound preparation disclosed by the invention have better compressibility and stability; the consumption of the accessory is reduced, so that the production cost is reduced; the quality of products is reduced; and the compound preparation is especially suitable for middle-aged groups suffering from rheumatic arthritis and groups whose moving joints are injured.
CN103265522A Lactone derivative derived from trichoderma citrinoviride and application thereof The invention relates to a lactone derivative derived from trichoderma citrinoviride and application thereof. The compound contains a molecular skeleton of hetero-oxygen atom pentacyclic lactone, and two methyls on the ring are located at the same side of the molecule. Verified by experiments, the lactone derivative has excellent anti-tumor activity. Besides, the lactone derivative can be applied to preparation of a cell proliferation inhibition drug or an anti-tumor drug and used for anti-tumor research.
CN102861069A Application of Houttuynoid B in medicine for treating laryngocarcinoma The invention discloses application of Houttuynoid B in preparation of a medicine for treating laryngocarcinoma, belonging to the technical field of new application of medicine. The invention discovers that Houttuynoid B has the remarkable inhibitory effects on the growth of human laryngocarcinoma cell strains including HEP-2, TU686, M2e and M4e through the evaluation of in vitro MTT antineoplastic activity. Therefore, Houttuynoid B can be used for preparing the anti-laryngocarcinoma medicine and has good development and application prospects. The application of Houttuynoid B in preparation of the medicine for treating laryngocarcinoma provided by the invention is disclosed firstly. The skeleton type belongs to new skeleton type, and the inhibitory activity of Houttuynoid B on laryngocarcinoma cells is unexpectedly strong.
WO2009140972A3 Modulation of the vps10p-domain receptors for the treatment of cardiovascular disease The present invention relates to methods for modulating the activity of one or more Vps10p-domain receptors selected from the group consisting of Sortilin, SorLA, SorCS1, SorCS2 and SorCS3, in an animal and methods for preparation of a medicament for the treatment of abnormal plasma lipid concentrations and associated diseases and/or disorders.The modulation is carried out by inhibiting or promoting the binding of ligands to the Vps10p-domain receptor. In vitro and in vivo methods for screening for agents capable of modulation of said Vps10p-domain receptor activity are also provided. The invention furthermore relates to methods of altering expression of said receptors in vivo.
WO2011059609A3 Dendrimer compositions and methods of synthesis The present invention relates to novel dendrimer compounds and methods of synthesizing the same. In particular, the present invention is directed to novel polyamidoamine (PAMAM) dendrimers, novel dendrimer branching units, methods for synthesizing such novel PAMAM dendrimers and functionalized dendrimers, as well as systems and methods utilizing the dendrimers (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease diagnosis and/or therapy, etc.))).
EP2310386A1 Benzoxazines, benzothiazines, and related compounds having nos inhibitory activity Disclosed are benzoxazines and benzothiazines of formula (I) wherein Q is O-(CHR6)1-3 or S-(CHR6)1-3; R1 and each R6 is H, optionally substituted [C1-6 alkyl, C1-4alkaryl, C1-4 alkheterocyclyl, C2-9 heterocyclyl, C3-8 cycloalkyl, C1-4 alkcycloalkyl] or - (CR1AR1B)nNR1cR1D wherein R1A, R1B, R1C, R1D are independently hydrogen, optionally substituted [C1-6 alkyl, C1-4alkaryl, C1-4 alkheterocyclyl, C2-9 heterocyclyl, C3-8 cycloalkyl, etc.] or wherein R1A and R1B combine to form =O, or wherein R1C and R1D combine to form an optionally substituted C2-9 heterocyclyl, and n is an integer between 1-6; each of R2 and R3 is H, hal, optionally substituted [C1-6 alkyl, C6-10aryl, C1-6alkaiyl, C2-9 heterocyclyl, C1-6 alkoxy, C1-6 thioalkoxy, (CH2)r2NHC(NH)R2A, CH2)r2NHC(S)NHR2A, C1-4 alkheterocyclyl] or hydroxy, wherein r2 is an integer from 0 to 2, R2A is optionally substituted [C1-6 alkyl, C6-10aryl, C^alkaryl, C2-9 heterocyclyl, C1-4 alkheterocyclyl,C1-6 thioalkoxy, C1-4 thioalkaryl, aryloyl, C1- 4thioalkheterocylyl, or amino]; each R4 and R5 is H, hal, (CH2)r2NHC(NH)R2A or CH2)r2NHC(S)NH R2A; Y1 and Y2 are together =O or Y1 and Y2 are independently H, optionally substituted [C1-6 alkyl, C6-10aryl, C1-6alkaryl, C2-9 heterocyclyl, C1-6 alkoxy, C1-6 thioalkoxy, C1-4alkheterocyclyl] or hydroxy; wherein only one of R2, R3, R4 and R5 is (CH2)r2NHC(NH)R2A or CH2)r2NHC(S)NH R2A; or a pharmaceutically acceptable salt or prodrug thereof. Said benzoxazines and benzothiazines of formula (I) inhibit nitric oxide synthase (NOS), particularly selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of formula (I), alone or in combinatioon with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.
CN1927181A Terbinafine nano milk-like liquid antifungal medicine and its preparation The invention discloses a terbinafine nanometer antifungal which is prepared by terbinafine, oil, surfactant, water according to the following method: First, the said raw materials are unloaded and weighed and reserved, then surfactants and oil is blended and mixed; terbinafine is added into cosurfactant and completely dissolved; the solution with terbinafine dissolved in it is added to the homogeneous mixed surfactant and oil, stirring uniform, finally, distilled water is slowly added dropwise, dropwising and stirring until the stable, homogeneous, transparent terbinafine nanometer antifungal is obtained. The drug with small particles, small viscosity, good fluidity and good nature stability, can reach through the skin and get into the blood circulation, inhibit squalene cycloxygenase, so as to treat the dermatophyte infection and many deep mycotic infection with a drastic therapeutic effect, and what is more the preparation of the invented products is simple, low energy consumption and without special equipment the drug can be mass produced.
CN1850033A Water soluble anti-cancer medicine slow-release fiber preparation and preparing method therefor The present invention relates to the field of medicine preparation, in the concrete, it relates to a show-released fibre preparation of water-soluble anti-cancer medicine for body implantation and its preparation method. It is characterized by that the fibre carrier is oil-soluble biological degradable material. and the medicine is water-soluble anticancer medicine, its medicine content is up to 15-50%.
WO2013024311A1 Amidoxime derivatives for the prevention and/or treatment of muscle atrophy The invention refers to the use of an amidoxime derivative of formula (I) or a pharmaceutically suitable acid addition salt thereof for the preparation of a pharmaceutical composition for the prevention and/or treatment of muscle atrophy.
US20110097399 Fast dissolving/disintegrating coating compositions A pharmaceutical composition for oral administration comprising a core and a film coating on the core that exhibits enhanced disintegration characteristics is disclosed. The film coating comprises a film forming polymer, an organic solvent, a super-disintegrant and, optionally, an acid labile material.
EP1956010A1 Bicyclical heterocycles, medicines containing these compounds, their application and method for their production Bicyclic heterocycle compounds (I) and their tautomers, stereoisomers and/or salts are new. Bicyclic heterocycle compounds of formula (I) and their tautomers, stereoisomers and/or salts are new. R1a : phenyl, 1-phenylethyl or indane-4-yl, where the phenyl nucleus is replaced by R 1>-R 3> group; R 1>, R 2>H, halo, 1-4C-alkyl-, OH-, 1-4C-alkoxy-, 2-3C-alkenyl-, 2-3C-alkynyl-, (hetero)aryl-, aryloxy-, arylmethyl-, arylmethoxy, heteroaryloxy-, heteroarylmethyl-, heteroarylmethoxy-, 1-3F substituted methyl, methoxy, CN-, NO 2- or NH 2, where aryl is phenyl or mono- or di substituted R 7>, where heteroaryl is pyridyl-, pyridazinyl-, pyrimidinyl-, pyrazinyl or mono- or disubstituted R 7>; R 3>H, F, Cl, Br, methyl or CF 3; R1b : azetidin-1-yl-, pyrrolidin-1-yl-, piperidin-1-yl-, homopiperidin-1-yl-, morpholin-4-yl-, homomorpholin-4-yl, piperazin-1-yl-, 4-(1-4C-alkyl-carbonyl)-piperazin-1-yl-, 4-(1-4C-alkyl-sulfonyl)-piperazin-1-yl-, homopiperazin-1-yl-, 4-(1-4C-alkyl-carbonyl)-homopiperazin-1-yl- or 4-(1-4C-alkyl-sulfonyl)-homopiperazin-1-yl-; R 4>mono-, di- or trisubstituted halo, 1-4C-alkyl-, 2-4C-alkenyl-, 2-4C-alkynyl-, 1-3F substituted methyl, methoxy, NH 2-, 1-4C-alkylamino-, di-(1-4C-alkyl)amino-, 1-4C-alkyl-carbonylamino-, N-(1-4C-alkyl)-1-4C-alkyl-carbonylamino-, 1-4C-alkyl-sulfonylamino-, N-(1-4C-alkyl)-1-4C-alkyl-carbonylamino-, amino-1-4C-alkyl-, 1-4C-alkylamino-1-4C-alkyl-, di-(1-4C-alkyl)amino-1-4C-alkyl-, 1-4C-alkyl-carbonylamino-1-4C-alky l-, N-(1-4C-alkyl)-1-4C-alkylcarbonylamino-1-4C-alkyl-, 1-4C-alkyl-sulfonylamino-1-4C-alkyl-, N-(1-4C-alkyl)-1-4C-alkyl-sulfo nylamino-1-4C-alkyl-, OH-, 1-4C-alkyloxy, 1-4C-alkyl-carbonyloxy-, hydroxy-1-4C-alkyl-, 1-4C-alkyloxy-1-4C-alkyl, 1-4C-alkyl-carbonyloxy-1-4C-alkyl-, 1-4C-alkyl-carbonyl-, CN-, 1-4C-alkyl-oxycarbonyl-, carboxy-, aminocarbonyl-, 1-4C-alkyl-aminocarbonyl-, di-(1-4C-alkyl)amino-carbonyl-, pyrrolidin-1-yl-carbonyl-, piperidin-1-yl-carbonyl-, piperazin-1-yl-carbonyl-4-1-4C-alkyl-piperazin-1-yl-carbonyl-, morpholin-4-yl-carbonyl-, 1-4C-alkylcarbonyl-1-4C-alkyl-, cyano-1-4C-alkyl-, 1-4C-alkyloxycarbonyl-1-4C-alkyl-, aminocarbonyl-1-4C-alkyl-, 1-4C-alkylaminocarbonyl-1-4C-alkyl-, di-(1-4C-alkyl)aminocarbonyl-1-4C-alkyl-, pyrrolidin-1-yl-carbonyl-1- 4C-alkyl-, piperidin-1-yl-carbonyl-1-4-alkyl-, piperazin-1-yl-carbonyl-1-4C-alkyl-, 4-1-4C-alkyl-piperazin-1-yl-carb onyl-1-4C-alkyl-, morpholin-4-yl-carbonyl-1-4C-alkyl-, 1-4C-alkylsulfanyl-, 1-4C-alkylsulfinyl-, 1-4C-alkylsulfonyl-, aminosulfonyl-, 1-4C-alkyl-aminosulfonyl-, di-(1-4C-alkyl)amino-sulfo nyl-, 1-4C-alkylsulfanyl-1-4C-alkyl-, 1-4C-alkylsulfinyl-1-4C-alkyl-, 1-4C-alkylsulfonyl-1-4C-alkyl-, aminosulfonyl-1-4C-alkyl-, 1-4C-alkyl-aminosulfonyl-1-4C-alkyl- or di-(1-4C-alkyl)amino-sulfonyl -1-4C-alkyl- (where the heterocyclic group is substituted by oxo); R1c : H, halo or 1-4C-alkyl (substituted by R 5>); R 5>OH, 1-3C-alkyloxy-, 3-6C-cycloalkyloxy-, amino-, 1-3C-alkylamino-, di-(1-3C-alkyl)amino-, bis-(2-methoxyethyl)-amino-, pyrrolidin-1-yl-, piperidin-1-yl-, homopiperidin-1-yl-, morpholin-4-yl-, homomorpholin-4-yl-, 2-oxa-5-azabicyclo[2.2.1]hept-5 -yl-, 3-oxa-8-aza-bicyclo[3.2.1]oct-8-yl-, 8-oxa-3-azabicyclo[3.2.1]o ct-3-yl-, piperazin-1-yl-, 4-1-3C-alkyl-piperazin-1-yl-, homopiperazin-1-yl-, 1-3C-alkyl-homopiperazin-1-yl-, formylamino-, 1-4C-alkylcarbonylamino-, 1-3C-alkyloxy-1-3C-alkyl-carbonylamino-, 1-4C-alkyloxycarbonylamino-, aminocarbonylamino-, 1-3C-alkylaminocarbonylamino-, di-(1-3C-alkyl)aminocarbonylamino-, pyrrolidin-1-yl-carbonylamino-, piperidin-1-yl-carbonylamino-, piperazin-1-yl-carbonylamino-, 4-1-3C-alkyl-piperazin-1-yl-carbonylam ino-, morpholin-4-yl-carbonylamino-, 1-4C-alkylsulfonylamino-, OH, 1-4C-alkoxy, 1-3F substituted methoxy- or ethyloxy-, 2-4C-alkyloxy (substituted by R 5>), 3-7C-cycloalkyloxy-, 3-7C-cycloalkyl-1-4C-alkyloxy-, tetrahydrofuran-3-yl-oxy-, tetrahydropyran-3-yl-oxy- or tetrahydropyran-4-yl-oxy, tetrahydrofuranyl-1-4C-alkyloxy- or tetrahydropyranyl-1-4C-alkyloxy- or 1-4C-alkoxy (substituted by R 6> substituted pyrrolidinyl-, piperidinyl- or homopiperidinyl); R 6>H, 1-3C-alkyl, 1-4C-alkoxy (substituted by morpholinyl), 1-3C-alkyl substituted pyrrolidinyl, piperidinyl, piperazinyl- or morpholinyl; and R 7>H, halo, 1-3C-alkyl-, OH-, 1-3C-alkyloxy-, -CF 2-, CF 3-, difluormethoxy-, trifluoromethoxy- or CN. An independent claim is included for the 8 preparations of (I). [Image] - ACTIVITY : Cytostatic; Respiratory-Gen; Gastrointestinal-Gen; Antipsoriatic; Antiinflammatory; Immunomodulator; Antianemic. - MECHANISM OF ACTION : tyrosine kinase-mediated signal transduction inhibitor; Epidermal growth factor receptor signal transduction inhibitor. The effect of (I) to inhibit epidermal growth factor receptor signal transduction was tested using non-radioactive cell proliferation assay. The result showed that 4-[(3-chloro-2-fluoro-phenyl)amino]-6-[trans-4-(morpholin -4-yl)-cyclohexyloxy]-7-methoxy-quinazoline exhibited the IC 5 0 value of 1 nM.
CN101601649B Ubenimex fat emulsion injection and preparation method thereof The invention discloses a ubenimex fat emulsion injection, comprising ubenimex, oil for injection, emulsifier, stabilizer, isoosmotic adjusting agent and water, wherein, the concentration of the ubenimex is 0.05-10g/ml, the concentration of the oil for injection is 5-30g/ml, the concentration of the emulsifier is 0.8-3.0g/ml, the concentration of the stabilizer is 0.1-2.0g/ml, and the concentration of the isoosmotic adjusting agent is 2-3g/ml. Through measuring, the quality and the appearance of the fat emulsion injection of the invention are uniform, the average particle diameter is about 300nm, and the pH value is 5.0-9.0, thus, the fat emulsion injection can be used for injection. The ubenimex fat emulsion injection has obvious anti-tumor function. According to the characteristics of common fat emulsion injection, the ubenimex fat emulsion injection as an anti-tumor medicine also has the functions of slow releasing, targeting, providing organisms with energy and the like.
CN102885834A Application of Gypensapogenin B to preparation of drug for fighting influenza A virus The invention discloses application of Gypensapogenin B to preparation of a drug for fighting influenza A virus. Experiments prove that Gypensapogenin B has remarkable inhibition effects on influenza A virus fluA, which indicates that Gypensapogenin B has potential application value in the field of treating influenza A virus infectious diseases. The application of Gypensapogenin B to preparation of the drug for fighting influenza A virus is firstly publicized; and as a framework type belongs to a brand-new framework type and has unexpectedly strong inhibitory activity on influenza virus without any possibility shown by other compounds, and has outstanding substantial characteristics and remarkable progress for controlling influenza virus infection at the same time.
US20110288020 Use of VEGF and homologues to treat neuron disorders The present invention relates to neurological and physiological dysfunction associated with neuron disorders. In particular, the invention relates to the involvement of vascular endothelial growth factor (VEGF) and homologues in the aetiology of motor neuron disorders. The invention further concerns a novel, mutant transgenic mouse (VEGFm/m) with a homozygous deletion in the hypoxia responsive element (HRE) of the VEGF promoter which alters the hypoxic upregulation of VEGF. These mice suffer severe adult onset muscle weakness due to progressive spinal motor neuron degeneration which is reminiscent of amyotrophic lateral sclerosis (ALS)—a fatal disorder with unknown aetiology. Furthermore, the neuropathy of these mice is not caused by vascular defects, but is due to defective VEGF-mediated survival signals to motor neurons. The present invention relates in particular to the isoform VEGF165 which stimulates survival of motor neurons via binding to neuropilin-1, a receptor known to bind semaphorin-3A which is implicated in axon retraction and neuronal death, and the VEGF Receptor-2. The present invention thus relates to the usage of VEGF, in particular VEGF165, for the treatment of neuron disorders and relates, in addition, to the usage of polymorphisms in the VEGF promotor for diagnosing the latter disorders.
US20110190254 Cephalosporin having catechol group The present invention provides Cephem compounds which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria as follows: A compound of the formula: wherein, X is N, CH or C—Cl; T is S or the like; A and G are lower alkylene or the like; B is a single bond or the like; D is a single bond, —NR7—, —CO—, —CO—NR7—, —NR7—CO—, —NR7—CO—NR7—, or the like; E is optionally substituted lower alkylene; F is a single bond or optionally substituted phenylene; R3, R4, R5 and R6 each is independently hydrogen, halogene, nitrile, or the like; or an ester, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.
US7175850 Formulation for topical non-invasive application in vivo A formulation comprising molecular arrangements capable of penetrating pores in a barrier, owing to penetrant adaptability, despite the fact that the average diameter of said pores is smaller than the average penetrant diameter, provided that the penetrants can transport agents or else enable agent permeation through the pores after penetrants have entered pores, characterized in that the formulation comprises at least one consistency builder in an amount that increases the formulation to maximally 5 Nm/s so that spreading over, and retention at, the application area is enabled and/or at least one antioxidant in an amount that reduces the increase of oxidation index to less than 100% per 6 months and/or at least one microbicide in an amount that reduces the bacterial count of 1 million germs added per g of total mass of the formulation to less than 100 in the case of aerobic bacteria, to less than 10 in the case of entero-bacteria, and to less than 1 in the case of Pseudomonas aeruginosa or Staphilococcus aureus, after a period of 4 days.
WO2006117760A1 Adrenergic receptor antagonists The present invention relates to α1a and/or α1b adrenergic receptor antagonists, which can be used to treat a disease or disorder mediated through α1a and/or α1b adrenergic receptors. Compounds and pharmaceutical compositions disclosed herein can be used to treat benign prostatic hyperplasia (BPH) and related symptoms thereof. Further, such compounds can be used to treat lower urinary tract symptoms that may or may not be associated with BPH. The present invention also relates to processes to prepare the disclosed compounds, pharmaceutical compositions thereof, and methods of treating BPH or related symptoms thereof.
EP1998767A2 Method for promoting composite tissue regeneration and uses thereof The present invention provides a use and method for GM284 to promote the regeneration of a bodily structure comprised of a composite tissue in a subject. Additionally, the present invention provides a use and method for GM284 to promote composite tissue regeneration in a subject. The present invention further provides a use and method for GM284 to promote the regeneration of cells of a composite tissue in a subject. Finally, the present invention provides a use and method for GM284 to treat an injury to a composite tissue in a subject in need of such treatment.
US20090226400 Continuous delivery methods for treating hepatitis virus infection The present invention provides methods of treating hepatitis virus infection. The methods generally involve administering an IFN-x by continuous delivery. Continuous delivery of IFN-x provides for a serum profile of IFN-x such that a sustained viral response is achieved.
CN103254174A Lansoprazole compound and pharmaceutical composition thereof The invention relates to a lansoprazole compound and a pharmaceutical composition thereof. The lansoprazole compound is a crystal. The characteristic peaks measured by X-ray powder diffraction are shown as 3.6, 4.8, 10.9, 14.0, 15.4, 16.9, 22.6, 24.7, 28.5, 32.1, 35.2, 36.7 and 39.3 at 2theta+/-0.2 degrees. The medical composition preparation comprises the lansoprazole compound. The preparation is in form of freeze-dried powder injections, troches, capsules, enteric-coated tablets or enteric-coated capsules. The lansoprazole compound prepared by the invention has better solubleness and stability. The lansoprazole pharmaceutical composition prepared by using the lansoprazole compound provided by the invention as the effective component is good in stability.
WO2006065751A3 Cpg oligonucleotide prodrugs, compositions thereof and associated therapeutic methods The present invention provides a CpG oligonucleotide prodrug that includes a thermolabile substituent on at least one nucleotide thereof. The present invention also provides compositions that include a carrier and a therapeutically effective amount of at least one CpG oligonucleotide prodrug. The present invention further provides therapeutic methods of using such thermolabile CpG oligonucleotide prodrugs and compositions thereof. The present invention further provides a method of inhibiting tetrad formation in a CpG oligonucleotide by functionalizing the CpG oligonucleotide with one or more thermolabile substituents.
US20080207669 (S)-N-Stereoisomers of 7,8-Saturated-4,5-Epoxy-Morphinanium Analogs Novel (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs and methods for their pharmaceutical uses are also disclosed. Such analogs are disclosed as being useful in treating, among varying conditions, hypermotility of the gastrointestinal tract.
US20110151017 Ophthalmic solutions with improved disinfection profiles The present invention relates to ophthalmic solutions with antimicrobial activity. The solutions have an antimicrobial compound such as hydrogen peroxide and a boron compound. In one embodiment, the solutions contain a boron compound such as sodium borate that provides antimicrobial activity in addition to that of hydrogen peroxide, particularly during periods following disinfection and neutralization of such solutions. This additional activity reduces the likelihood of microbial growth in contact lens disinfection applications that neutralize hydrogen peroxide.
US20080031957 Pulmonary delivery of 1alpha,25-dihydroxyvitamin D3 and co-administration of parathyroid hormone or calcitonin Pharmaceutical pulmonary compositions, methods of delivery to the lungs of a human and methods of treatment thereof. Pharmaceutical formulations including 1α,25-dihydroxyvitamin D3, an alcohol such as ethanol, and a polyol such as propylene glycol. Another pharmaceutical pulmonary formulation includes 1α,25-dihydroxyvitamin D3 and dry bulking powder, which is used in a dry powder inhaler. Another pharmaceutical formulation includes 1α,25-dihydroxyvitamin D3 and an aerosol propellant, which is used in a metered dose inhaler. The pharmaceutical pulmonary formulations may include a second active pharmaceutical ingredient such as calcitonin or a N-terminal peptide fragment of parathyroid hormone consisting of the first 34 to 38 amino acids of SEQ ID No. 1. Pulmonary delivery of the formulations efficaciously increase serum calcium levels in mammals, manage hypocalcemia, treat calcium metabolic disorder and reduce elevated parathyroid hormone levels.
US20100216820 Thienopyrimidiones for treatment of inflammatory disorders and cancers The current invention provides compounds of formula (1): wherein: one of Q1, Q2 and Q3 is S, and the other of two of Q1, Q2 and Q3 are —CR1—, which are inhibitors of PI3K-delta. These compounds are useful for treatment of conditions mediated by PI3K-delta, such as hematopoietic cancers, immune disorders, and bone resorption disorders. The invention further provides pharmaceutical compositions comprising a compound of formula (1) and methods of using these compounds and compositions to treat conditions mediated by PI3K-delta.
US7759364 Method for producing non-hydrated fexofenadine hydrochloride and a novel crystalline form obtained thereby The invention relates to non-hydrated fexofenadine hydrochloride which can be obtained from a fexofenadine base and hydrogen chloride, according to the reaction conditions, either in the form of a novel polymorph (“form A”), in an amorphous form, or in the form of a mixture of different polymorphs. Said novel polymorph (“form A”) can be used as a therapeutic active ingredient and can be processed to form a pharmaceutical containing the same and a pharmaceutically acceptable carrier. Said pharmaceutical is suitable for use as an antihistaminic agent, an antiallergic agent and/or a bronchodilating agent.
CN101091712A Application of 9 ¿C (2 ¿C hydroxyethoxy methyl) in preparing silkworm drug The present invention relates to an application of 9-(2-hydroxyethoxymethyl) guanine, in the concrete, it relates to an application of 9-(2-hydroxyethoxymethyl) guanine in preparation of medicine for preventing and curing domestic silkworm diseases. The tests show that said medicine can obtain obvious effect for preventing and curing nuclear polyhedral virus (NPV) disease of domestic silkworm. Its medicine effect is stable and reliable.
US20050289658 System for regulating in vivo the expression of a transgene by conditional inhibition The present invention relates to novel constructs and compositions and to a novel method for regulating the expression of a transgene of interest in vivo by conditional inhibition, and to the uses thereof in experimental, clinical and therapeutic domains or for the production of animals or plants. For example, the novel regulation method is based on the coexpression of a transgene of interest encoding a transcript of interest and of an inhibitory transgene encoding an inhibitory transcript specific for the transcript of interest, so as to obtain constitutive inhibition of the activity of the transcript of interest, and to be able to ensure effective regulation of the transcript of interest, either by inhibiting its inhibitory transcript, or by activating the transcript of interest, or alternatively by activating the transcript of interest and concomitantly inhibiting its inhibitory transcript.
EP1689249A1 Dietary non-essential amino acid tyrosine regulates the body weight of animals through regulating the animal appetite or food intake The invention develops a weight management system which comprises administering tyrosine in the desired amount to change and maintain the body weight of an animal. If the animal is overweight, the animal would be fed a low level tyrosine food composition. If the animal is underweight, the animal would be fed a high level tyrosine food composition. The invention also relates to an low tyrosine animal food which contains, on dry matter basis: ( a) from about 0.01 % to less than about 0.4% of tyrosine, (b) from about 0.42% to about 3% of phenylalanine (c) from about 7% to about 70% of protein, (d) from about 1 % to about 60% of fat, (e) from 0 to 90% of carbohydrate, (f) from 0 to about 40% of dietary fiber, and (g) from 0 to about 15% of nutritional balancing agents.
CN101352413A Compound anticancer sustained-release injection containing clofarabine The invention discloses a clofarabine compound anticancer slow-release injection which is an anticancer slow-release injection and consists of slow-release microspheres and solvent; wherein, the slow-release microspheres comprise anticancer effective ingredients and slow-release auxiliary materials; the solvent is a special solvent containing a suspending agent; the anticancer effective ingredients are combination of the clofarabine and a clofarabine synergist which is selected from antitumor antibiotics and/or antimetabolic drugs; the slow-release auxiliary materials are selected from one or combination of copolymer of racemic polyactic acid and copolymer thereof, copolymer of monomethyl polyethylene glycol or polyethylene glycol or carboxyl-terminated polyactic acid and polyactic acid, copolymer of bi-fatty acid and sebacic acid, poly-(erucic acid dimmer-sebacic acid), poly-(fumaric acid-sebacic acid), polifeprosan and EVAc; the suspending agent has 80cp-3000cp of viscosity; the slow-release microspheres also can be made into a slow-release implant, is injected or placed in tumor or around the tumor, and release drugs for about 40 days; the slow-release injection and the slow-implant can be applied separately so as to suppress the tumor growth or is applied with the non-operative treatment of chemoradiotherapy, and the like, in a combining way, so as to enhance the curative effect thereof significantly.
WO2008124209A1 1,3,8-trisubstituted-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as ligands of the orl-i receptor for the treatment of anxiety and depression The present invention is directed to novel 1.3.8-trisubstituted-1.3,8-triaza-spiro[4:5]decan-4-one derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor. R3 is selected from the group consisting of R0 is selected from the group consisting of -CCH, hydroxy, -N3, -O-C(0)-C1-4 alkyl, -O-SO2-C1-4 alkyl, -O-(2- tetrahydropyranyl); wherein R1 is 1-aceπaρhthenyl; R2 is 4-fluorophenyl; A1 is selected from the group consisting of -CH2-,-CH2CH2-,-CH2CH2- and -CH2CH2CH2CH2
US20090176793 3-(l,3-BENZODIOXOL-5-YL)-6-(4-CYCLOPROPYLPIPERAZIN-l-YL)-PYRIDAZINE, ITS SALTS AND SOLVATES AND ITS USE AS HISTAMINE H3 RECEPTOR ANTAGONIST 3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine and salts and solvates thereof, (I) having histamine H3 antagonistic activity can be used in pharmaceutical compositions.
US20120259187 Dynamic colorectal pdt application Dynamic colorectal PDT methods, devices and photosensitizer compositions to treat abnormal cell growth in anal tissue such as perianal and intra-anal intraepithelial neoplasia grade III are presented. Dynamic colorectal PDT method comprises the steps of administering topically, intravenously or orally a photosensitizer composition; irradiating; monitoring treatment parameters before, during and/or after irradiation. Photosensitizer composition comprises Temoporfin and excipients/carriers, appropriate for the application method. An applicator is provided for colorectal PDT treatments enhancing irradiation delivery and monitoring treatment parameters. Preferably, applicator is made of a material, used to monitor the fluence rate simultaneously while doing optical spectroscopy. Measurement probe devices are provided for monitoring PDT treatment parameters in-vivo. A device for colorectal PDT treatment is also provided, comprising laser radiation source operating at about 400 and 800 nm; excitation laser radiation source operating at about 650 nm for fluorescence measurements; multichannel dosimetry device; long pass filter; waveguides and measurement probes.
CN103211770A Igutimod slow release multielement composition and preparation method thereof The invention belongs to the pharmaceutical field, relates to an igutimod slow release multielement composition and a preparation method thereof, and in particular relates to a medical slow release multielement composition prepared by using igutimod as the active component and a framework carrier material and a release adjustor as a carrier. A plasticizer is added if necessary to reduce the extruding temperature and simplify the extruding process. The preparation method is a thermal melting extruding method which is simple in process and easy for industrial production, and is not involved in organic solvents. The slow release multielement composition consists of severe of dozens of slow release particles which are uniform in grain size, so that the composition is high in safety.
CN1615859A Nimodipine adhesive sheet The nimodipine plaster belongs to the field of medicine preparation form design, and consists of back lining film, medicine library layer, release controlling film, pressure-sensitive glue layer and protecting film. The medicine library layer is cross-linked polymer film containing nimodipine 10-20 wt% and transdermal osmosis promoter 2-10 wt%, and has thickness of 1.0-1.5 mm. The pressure-sensitive glue layer is cross-linked polymer film containing nimodipine 1-3 wt%, and has thickness of 0.05-0.3 mm. Animal experiment shows that after the nimodipine plaster is applied once on chest, steady medicine concentration in blood may be maintained for about one week. The present invention has obviously raised bioavailability of nimodipine and skin irritation and irritability within relevant stipulations.
CN102302460A Methylprednisolone sodium succinate freeze dried powder injection and preparation method thereof The invention discloses methylprednisolone sodium succinate freeze dried powder injection and a preparation method thereof. The methylprednisolone sodium succinate freeze dried powder injection in each syringe consists of 633.7 mg of succinic methylprednisolone, 112 mg of NaHCO3, 6.4 mg of NaH2PO4.H2O and 69.6 mg of Na2HPO4 which are dissolved in water for injection till 5 ml, and the powder injection is obtained after filling and freeze drying.
US6984651 Piperidine amides as modulators of chemokine receptor activity The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
CN1771968A Ursolic acid fat emulsion injection and its prepn The present invention relates to one kind of ursolic acid fat emulsion injection and its preparation. The fat emulsion consists of ursolic acid as active component and medicinal supplementary material, and consists of ursolic acid 0.01-0.15 wt%, oil for injection 5-30 wt%, emulsifier 1-9 wt%, solubilizer 1-6 wt%, isosmotic agent 2-2.5 wt%, and antioxidant 0.01-0.03 wt%, except water for injection. The present invention has simple preparation process, and the injection may be used clinically in intravenous injection, and has high bioavailability, high stability, raised treating effect, slow releasing and targeting effect, and energy providing effect.
US20110281933 Methods and compositions for the management of cardiovascular disease with oligonucleotides Disclosed are compositions and methods for treating cardiovascular disease and reducing the adverse effects induced by the administration of statins. In particular, disclosed is the use of antisense compounds to augment the expression of mirR-33 and associated genetic elements. In particular methods of the treatment of cardiovascular disease and the modulation of miR-33 levels is disclosed as well as treatment of the secondary effects including cholestasis, induced by the administration of statins is disclosed. Also disclosed is the treatment of Benign Recurrent Intrahepatic Cholestasis and reverse cholesterol transport. The disclosed methods and compositions may be practiced separately or co-administered with satins to reduce or treat statin induced secondary effects.
EP1324761B1 Uridine therapy for patients with elevated purine levels The invention is based on the discovery that patients having elevated purine levels, e.g., individuals diagnosed with pervasive developmental disorders, such as autistic disorder, and/or neuromuscular disorders, can be treated with uridine compositions.
WO2009067790A1 STIMULATION OF HYPOXIA INDUCIBLE FACTOR -1 ALPHA (HIF-1α) FOR THE TREATMENT OF CLOSTRIDIUM DIFFICILE ASSOCIATED DISEASE (CDAD), FOR INTESTINAL MOTILITY AND FOR DETECTING INFECTION The present application relates to methods and compositions for treating Clostridium difficile-associated disease (CDAD) by administering an agent that increases hypoxia-inducible factor 1α (HIF-1 α) levels. The agent is selected from the group consisting of a C. Difficile toxin, TcdA, TcdB, an inhibitor of prolyl hydroxylase, dimethyloxalyl glycine (DMOG) and HIF- 1α protein itself. While it is known that C. difficile toxins can induce inflammatory events that are associated with CDAD, the specific role of HIF-1 has not been studied in CDAD. The present inventors have determined that HIF-lα is induced by C. Difficile toxins. The inventors have shown that HIF-1α activation has a protective effect in CDAD. The inventors have also shown that HIF-lα activation increases ileal smooth muscle contraction.
WO2014078446A3 Skin wound healing and scar reduction with prostaglandin ep4 agonist combinations A combination of a prostaglandin EP4 agonist and an effective amount of : a prostaglandin EP2 agonist, a skin growth factor, a small peptide, a small inhibitory RNA targeting excess chronic inflammation or fibrosis, a cytokine with beneficial anti-inflammatory activity, an adenosine A2a receptor agonist, an anti-oxidant, or a combination thereof, may be used to treat skin wounds or scars.
US20080227847 (S)-2-hydro-2,6-diaminohexanal-(E)-methoxy-4-oxobut-2-enoate(lysine monomethylfumarate); treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders The present invention relates to novel amino acid salts of fumaric acid monoalkylesters. The salts are suitable for use as active substances in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders.
EP2376633A1 Antisense compositions and methods for modulating contact hypersensitivity or contact dermatitis Provided are methods and compositions, including topical compositions, for inducing tolerance to a sensitizing agent known to provoke contact hypersensitivity in a subject. Included are methods of topically applying to the subject an effective amount of an antisense composition targeting the start site or splice site of a CFLAR mRNA.
US7326427 Tablet composition containing Kampo medicinal extract and its manufacturing process A Kampo medicinal extract-containing tablet composition contains a Kampo medicinal extract powder, cellulose glycolate and sodium hydrogen carbonate. It preferably further contains silicic anhydride. A process to manufacture a Kampo medicinal extract-containing tablet composition by the step of adding silicic anhydride and water to a Kampo medicinal extract powder, stirring and granulating the mixture, and the step of mixing the granulated substance with cellulose glycolate and sodium hydrogen carbonate. The Kampo medicinal extract-containing tablet composition can be satisfactorily disintegrated and dissolved and a process for manufacturing the same, by formulating specific compounds to a Kampo medicinal extract powder.
CN102217712A Pinene-containing feed or feed additive The invention relates to pinene-containing feed or a feed additive for preparing the feed, wherein the feed or the feed additive contains the effective dose of pinene, in particular to alpha-pinene, at least one phellandrene preferentially, which is used as an agent for economic animal synergism and flavor improvement. By adopting the feed or the feed additive, not only the health of animals can be promoted, the occurrence of respiratory system diseases of the animals can be reduced and the utilization efficiency of the animal feed can be significantly improved, but also the flavor of animal products can be improved. A product of the invention is derived from the non-edible parts of human edible plants, thereby not only fully utilizing existing plant resources, but also being capable of producing safe and healthy livestock products, thereby being an ideal substitute product of the antibiotic feed additive.
EP2145615A1 Skin-lightening agent containing equol compound as active ingredient An object of the present invention is to provide a whitening agent containing a novel whitening substance as an effective ingredient. The above object is attained by providing a whitening agent containing equol and/or equol glycoside, in which one or more glycosyl groups bind to the hydroxyl group(s) of equol, as an effective ingredient.
CN1895252A Zirasitone mesylate soluble medicinal preparation An aqueous solution type Qilaxitong methanesulfonate is composed of the anhydrous 5-[2-[4-(1,2-benzoisothiazole-3-yl)-1]-piperazinyl]-6-chloro-1,3-bihydro-indole- 2-ketone methanesulfonate, at least one pharmacologically acceptable aqueous solution of polyol, and the pharmacologically acceptable auxiliary.
WO2011076784A3 New inhibitors of cyclophilins and uses thereof The present invention relates to a compound of formula (I): Formula (I), wherein: - n is 0, 1 or 2; - A is in particular CH or N; - X is in particular CO, SO2, CS, and R1 is in particular H, - R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, - R6 is in particular H or an alkyl group, and - R7 is in particular an aryl group, substituted with at least one NH2 group for its use in the prevention and/or the treatment of viral pathologies or infections.
CN101280326A Preparation and application of compound for inhabiting aspergillus fumigatus activity The invention relates to a methyl asterrate preparation method and the application thereof. The solid fermentation is performed to Fungi Geomyces sp, chemical compound methyl asterrate can be obtained by performing purification to fermentation products, and the chemical compound methyl asterrate prepared by the invention is confirmed methyl asterrate by applying technologies such as mass spectrum, nuclear magnetic resonance spectrum and infrared spectrum and documents. The invention also provides usages of the chemical compound in preparing drugs which can restraint the activity of aspergillus fumigatus.
US20060003975 Combination of an aldosterone receptor antagonist and an HMG CoA reductase inhibitor Novel methods and combinations for the treatment and/or prophylaxis of a pathologic condition in a subject, wherein the methods comprise the administration of one or more HMG Co-A reductase inhibitors and one or more aldosterone receptor antagonists, and the combinations comprise one or more HMG Co-A reductase inhibitors and one or more of said aldosterone receptor antagonists.
CN101822656A Application of curcumin The invention discloses an application of curcumin in the preparation of medicines for curing erectile dysfunction. The curcumin unit dose is 5-800mg. pharmacodynamics experiments and clinical experiments prove that the medicine of the invention has the advantages of low side effect and wide therapeutic window; after taken, the medicine can not generate after effect on patients, the medicine has the characteristics of the natural medicine; and the medicine of the invention has good pharmacological effects.
CN101264082B Compound for treating gastric injury The invention discloses a purpose of a structural formula I compound in preparing the medicine used to prevent or cure stomach trauma of mammals; wherein, the medicine can be prepared into an orally administered dosage form, which can be selected from pill, capsule, powder, grain, crystal, solution, suspension, soup, syrup, elixir, tea and masticatory; moreover, the medicine can also be prepared into a skin-penetrating or locally administered dosage form, which can be any one of suspension, gel, ointment, cream, emulsion, and powder.
EP2550360A1 Bivalent antisense oligonucleotides The present invention provides bivalent molecules comprising a first oligonucleotide linked to a second oligonucleotide. The first and the second oligonucleotide are preferably linked via a linking moiety. Preferably, both the first and/or the second oligonucleotide comprise an antisense sequence complementary to a cellular RNA such as mRNA or microRNA.
WO2014128240A1 Inhibitors of na(v) 1.9 channel activity and uses thereof for treating pain The present invention relates to novel compounds for use for preventing, alleviating or treating pain in a subject. Also herein described are pharmaceutical compositions, their preparation and uses as well as methods for preventing, alleviating or treating pain using such compounds and compositions.
CN101785768A Bactericide for rabbits The invention designs a bactericide for rabbits. The bactericide mainly comprises water and ethanol and 1-[(2- chlorphenyl)diphenylmethyl]-1H-imidazole which are added into the water, wherein the ratio of the 1-[(2- chlorphenyl)diphenylmethyl]-1H-imidazole(g) to the ethanol(ml) to the water(ml) is 1:250-550:200-350. The bactericide for rabbits of the invention is colorless or yellowish solution, mainly used for fungus prevention of newborn rabbits and is externally used. The detailed blending ratio of raw materials is provided in the invention, and according to the blending ratio, the bactericide for rabbits can achieve a perfect price-to-performance ratio of a prevention effect to the cost of raw materials, and the effective rate of preventing the breeding of fungi is over 99 percent; and simultaneously, because the bactericide for rabbits is externally used, the bactericide for rabbits can effectively block routes of infection while killing fungi on the outer surfaces of infected rabbits, so that the aim of preventing dermatomycosis of rabbit herds is fulfilled.
CA2183543C Sexual steroid-containing transdermal therapeutic systems Transdermal therapeutic systems that contain sex steroids and optionally penetration-enhancers and crystallization inhibitors are described, which are characterized in that they contain dimethyl isosorbide, with the exception of systems that contain active ingredient-containing, non-free-flowing gel phases or 3-keto-desogestrel.
US7470685 e.g. 1-(2-(4-(N'-(3-Methyl-benzylidene)-hydrazino)-6-morpholin-4-yl-pyrimidin-2 -yloxy)-ethyl)-1H-pyridin-2-one; control interleukin production; antiinflammatory, antidiabetic agent; interleukin IL-12 overproduction-related disorder: rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Re m; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C═N—Rc, C═N—ORc, C═N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl, alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
CN102988380A Application of Houttuynoid B to preparation of medicine for rising white blood cells The invention relates to a new application of a compound Houttuynoid B in the field of pharmacy, and particularly relates to an application of Houttuynoid B to preparation of a medicine for rising white blood cells, which is made public for the first time. As a framework type is brand-new, and the inhibitory activity of the Houttuynoid B to low white blood cells is unexpectedly strong, the possibility of obtaining any revelation from other compounds does not exist, and the Houttuynoid B has remarkable substantive distinguishing features and obviously has a notable progress to prevention and treatment of the low white blood cells.
EP1142885B1 2-(n-cyanoimino)thiazolidin-4-one derivatives Novel 2-(N-cyanoimino)thiazolidin-4-one derivatives represented by general formula (I), which exhibit excellent cholesterol-lowering and triglyceride-lowering activities and are useful in the prevention or treatment of hyperlipidemia and diseases resulting therefrom.
WO2009156082A1 Oxazolidinones for the treatment of chronic obstructive pulmonary disease (copd) and/or asthma The present invention relates to the use of selective inhibitors of coagulation factor Xa, in particular of oxazolidinones of the formula (I), for the treatment and/or prophylaxis of asthma and/or chronic obstructive pulmonary disease and/or disorders related to asthma and/or chronic obstructive pulmonary disease (COPD) such as thromboembolic events (including e.g. pulmonary embolism (PE), arterial and venous thrombosis, myocardial infarction, stroke) as well as their use for the preparation of pharmaceutical drugs for the treatment and/or prophylaxis of asthma and/or chronic obstructive pulmonary disease and/or disorders related to asthma and/or chronic obstructive pulmonary disease such as thromboembolic events.
CA2301874C Suppression of malignancy utilizing ribonucleotide reductase r1 The present invention provides a method of modulating the malignant properties of a cell in a human or other mammal by contacting a neoplastic cell with a growth modulating amount of an expressible nucleic acid sequence for ribonucleotide reductase R1 of the mammal. The present invention also provides and uses a growth modulating amount of the ribonucleotide reductase R1 protein or biologically active peptide to modulate the malignant properties of a cell in a human or other mammal. The method provides for a generally elevated expression of the R1 component of mammalian ribonucleotide reductase. The expressible nucleic acid sequence can be in the form of a vector for gene therapy.
EP1554381A2 Post transcriptional silencing by short interfering rnas The present invention relates to synthesised RNAs, more specific short interfering RNAs (siRNAs) that are able to modulate the expression of Tissue Factor (TF), as well as to a pharmaceutical preparation comprising the synthesised siRNA(s) and use thereof.
CN101269050A Acidum citricum nolvadex capsule and preparation method thereof The invention discloses a citric acid tamoxifen capsule and consists of 5 to 25 percent of citric acid tamoxifen, 35 to 55 percent of starch, 35 to 50 percent of microcrystalline cellulose, 2 to 5 percent of PVPP and 0.2 to 0.5 percent of magnesium stearate according to the weight percentage.
CN101244064B Pharmaceutical combination for preventing and treating motion sickness and preparations thereof The invention relates to a drug composition for the treatment of motion sickness, as well as the preparation, wherein the drug composition comprises caffeine and chlorpheniramine maleate; 50 to 500 mg caffeine and 2 to 20 mg chlorpheniramine maleate are contained in each preparation unit; the preferred mass ratio of caffeine to chlorpheniramine maleate in each composition is 50:2 and the preferred amount of each component is 200 mg caffeine and 8mg chlorpheniramine maleate. The drug composition has an advantage of effectively treating and preventing motion sickness without side effect of sleepiness or lassitude; besides, conventional adjuvant can be added in the drug composition to make drugs through any conventional method for motion sickness treatment; controlled release technologies can also be adopted to make controlled release preparations.
CN102816184A (2-(2-oxyl-4-sulfo-pyrimidine) ethyoxyl) methyl-phosphonate derivatives as well as preparation method and applications thereof The invention discloses (2-(2-oxyl-4-sulfo-pyrimidine) ethyoxyl) methyl-phosphonate derivatives as well as a preparation method and application thereof. The derivatives have the structure shown in a general formula (I), wherein R1 is hydrogen, methyl, allyl, propargyl or benzyl; and R2 is hydrogen, ethyl, trimethylacetic acid methyl, isopropoxy ketonic oxygen methyl or benzyloxy-ketonic oxygen methyl. The invention also provides a preparation method and applications of the derivatives. The derivatives have higher a hepatitis B virus (HBV) activity inhibition effect, and can be used as a lead compound to be used for preparing medicines for resisting HBV (Hepatitis B Virus).
WO2013149977A1 1,2- pyridazine, 1,6- pyridazine or pyrimidine - benzamide derivatives as gpbar1 modulators This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula I wherein B1 to B3 and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
US8226957 Methods of preventing and treating respiratory viral infection using immunomodulatory polynucleotide sequences The invention provides methods of preventing and/or treating infection by a respiratory virus such as respiratory syncytial virus (RSV), particularly reducing infection and/or one or more symptoms of respiratory virus infection. A polynucleotide comprising an immunostimulatory sequence (an “ISS”) is administered to an individual which is at risk of being exposed to a respiratory virus, has been exposed to a respiratory virus or is infected with a respiratory virus. The ISS is administered without any antigens of the respiratory virus. Administration of the ISS results in reduced incidence and/or severity of one or more symptoms of respiratory virus infection.
CN102600135A Application of compound celecoxib in preparing information therapeutic medicament as well as preparation method thereof and novel medicine prepared by using compound The invention discloses an application of compound celecoxib in a preparing information therapeutic medicament as well as a preparation method thereof and a novel medicament prepared by using the compound. The information therapeutic medicament is not directly contact with a human body during treatment, the substance element of the medicament is not consumed, the medicine information is only utilized for physiotherapy, the effect of chemotherapy is achieved, the treatment windows are expanded by more than 1000 times, and the side effects of the chemotherapy are avoided. The celecoxib is used as the information therapeutic medicament, the content of an active ingredient is not changed, and the information therapeutic medicament can be effectively used as a chemotherapy general preparation for secondary use.
CN101428027B Medicament composition for preventing and treating thrombosis The invention relates to pharmaceutical composition used for preventing and treating the disease of thrombosis and a preparation method thereof, and the usage of the composition in treatment of thrombosis associated disease. The composition comprises the components of arecoline, ligustrazine and paeonol.
WO2008101665A1 Macrocyclic compounds as hcv ns3 protease inhibitors The present application describes macrocyclic compounds of formula (I) with NS3 protease inhibitory activity for treating hepatitis C virus infection.
DE102005019458A1 Composition, useful in the preparation of pellets and the multi-particular-presentation form, comprises cefuroximaxetil and carrageenan of the group of lambda carrageenan, tau carrageenan and kappa carrageenan Composition comprises cefuroximaxetil and at least one carrageenan of the group of lambda carrageenan, tau carrageenan and kappa carrageenan. Independent claims are included for: (1) preparation of pellets from the composition comprising mixing the cefuroximaxetil, the carrageenan and optionally further content material, preferably tri calcium phosphate and/or sucrose ester, granulating the obtained product, extruding the granulated mixture, optionally spheronizing the extruded mixture and optionally covering the obtained pellets with a gastric juice resistant and/or saliva resistant coat; (2) the pellets, which are obtained by the procedure; (3) a multi-particular, presentation form comprising the composition or the pellets; (4) a presentation system comprising the presentation form in a straw with at least one barrier device to the unique dispensation; (5) a kit from the presentation form and a physiologic compatible transportation liquid with a pH value of =6; (6) a crystalline cefuroximaxetil exhibiting a roentgen diffraction spectrum of 8.3, 10.4, 13, and 25.5 (+-0.2 [deg]2theta ); and (7) a composition comprising amorphous cefuroximaxetil and crystalline cefuroximaxetil, preferably the alpha modification, where the weight ratio is 90:10 to 10:90. - ACTIVITY : Respiratory-Gen; Antimicrobial; Uropathic.
CN1872056A Compound preparation of amoxicillin and bromhexine HCL suitable to application of children, prescription and preparation method A compound medicine in the form of powder or dried suspended mixture suitable for children is prepared from amoxycillin, bromhexine hydrochloride and the pharmacologically acceptable auxiliaries including flow assistant lubricant, high-molecular polymer, sweetener and fragrant flavouring. Its preparing process is also disclosed.
EP1996541A1 2-(aryloxy)acetamide factor viia inhibitors useful as anticoagulants The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R7, R8, and R9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.
US20090082363 Deuterium-enriched posaconazole The present application describes deuterium-enriched posaconazole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20100284961 MCP-1 binding nucleic acids The present invention is related to a nucleic acid, preferably binding to MCP-1, selected from the group comprising type 1A nucleic acids, type 1B nucleic acids, type 2 nucleic acids, type 3 nucleic acids, type 4 nucleic acids and nucleic acids having a nucleic acid sequence according to any of SEQ. ID. No. 87 to 115.
EP2468747A1 2-Selenophene-4-quinolones as anticancer agents The present application is directed to 2-selenophene 4-quinolones, which exhibit significant anticancer activities.
EP1904514A2 Crystalline forms of ciclesonide The invention encompasses a crystalline form of ciclesonide characterized by an XRD pattern having peaks at about 1 1.0, 14.8, 15.7, 16.5, and 22.8 degrees two-theta ± 0.2 degrees two-theta, methods of its preparation and pharmaceutical compositions thereof. Formula (I).
WO2011040048A1 Virus inactivation sheet Disclosed is a virus inactivation sheet that can inactivate viruses adhering to said sheet regardless of the existence of an envelope, or the presence of lipids or proteins. The virus inactivation sheet can inactivate viruses adhering thereto, and is characterised by having a sheet body, and univalent copper compound microparticles and/ or iodide microparticles retained on the sheet body. The virus inactivation sheet can inactivate a variety of viruses and can inactivate said viruses even in the presence of lipids and proteins.
CN1962615A Diamine compound for resisting hepatitis B virus and its preparation method and its application The invention discloses a diamine compound of anti-hepatitis B virus and preparing method and application with structure as formula (I), which is characterized by the following: adopting compound in the structural formula (II) as raw material; oxidizing directly; fitting for preparing the drug to prevent or treat relative disease of anti-hepatitis B virus.
US20130040899 Use of PEDF-Derived Polypeptides for Treating Liver Cirrhosis The present disclosure elucidates that 34-mer PEDF suppresses hepatic stellate cells (HSCs) from activation by diminishing the levels of alpha-smooth muscle actin (α-SMC), collagen type 1, and monocyte chemoattractant protein-1 (MCP-1); and 44-mer PEDF promotes liver regeneration process by enhancing the replication of liver-derived progenitor cells (LDPCs). Accordingly, methods and compositions directing to the new use of the 34-mer PEDF or 44-mer PEDF in patients suffering from liver cirrhosis are provided herein.
CN103565773A Pharmaceutical composition of prasugrel hydrochloride The invention discloses a composition containing prasugrel hydrochloride and a preparation method of the composition. The composition contains 2-10 parts of prasugrel hydrochloride and a pharmaceutically acceptable carrier, wherein the carrier consists of 10-89 parts of one or more pharmaceutically acceptable fillers, 1-10 parts of one or more pharmaceutically acceptable binding agents, 2-10 parts of one or more pharmaceutically acceptable disintegrating agents and 1-10 parts of one or more pharmaceutically acceptable lubricating agents; the preparation method comprises the steps of premixing, implementing dry granulation, grinding through a grinding machine, mixing, and optionally tabletting, coating and packaging. The preparation method can provide a prasugrel hydrochloride tablet which is quick to release and stable as well as other dosage forms thereof.
US7087587 Blending with adjuvants, compression, coating The present invention provides a process for the preparation of tablets comprising S-adenosylmethionine and/or a pharmaceutically and/or dietarily acceptable derivative thereof by blending that active component with specified additives, compressing the blend, followed by coating.
WO2007002051A1 Carboline derivatives and their use as inhibitors of flaviviridae infections The present invention relates to compounds that are useful in the treatment or prophylaxis of viruses belonging to Flaviviridae, such as a flavivirus, a pestivirus, or a hepacivirus, particularly dengue fever, yellow fever, West Nile virus, or HCV.
WO2010018352A1 Heterocyclic compounds used in the treatment of diseases where enhanced m3 receptor activation is implicated The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in in the treatment of diseases where enhanced M3 receptor activation is implicated.
US20050256112 Enhancing the serotonergic neurotransmission; side effects reduction; nervous system disorders; sexual disorders; analgesics; antidepressants; anticancer; anxiolytic agents; neurodegenerative diseases; gastrointestinal tract disorders; eating disorders The present invention relates to a pharmaceutical composition for treating, for example, a disorder or condition selected from the group consisting of hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress disorder, avoidant personality disorder, sexual dysfunction, eating disorders, obesity, chemical dependencies, cluster headache, migraine, pain, Alzheimer's disease, obsessive-compulsive disorder, panic disorder, memory disorders, Parkinson's diseases, endocrine disorders, cerebellar ataxia, gastrointestinal tract disorders, negative symptoms of schizophrenia, premenstrual syndrome, Fibromyalgia Syndrome, stress incontinence, Tourette syndrome, trichotillomania, kleptomania, male impotence, cancer, chronic paroxysmal hemicrania and headache in a mammal, preferably a human, comprising (i) an atypical antipsychotic or a pharmaceutically acceptable salt thereof, (ii) a 5-HT1B receptor antagonist or a pharmaceutically acceptable salt thereof, wherein the 5-HT1B receptor antagonist is selected from the group consisting of (A) a compound of the formula I as described in the specification and (B) a compound of the formula II as described in the specification, and optionally (iii) a pharmaceutically acceptable carrier.
CN103421010A Pteridinone derivative as EGFR inhibitor and application thereof The invention relates to a pteridinone derivative as an epidermal growth factor receptor tyrosine kinase (EGFR) inhibitor and an application thereof. Specifically, the invention relates to the compound represented by the following formula I, a pharmaceutical composition containing the compound represented by the following formula I, and the application of the compound in preparation of a drug for treating EGFR mediated diseases or inhibiting EGFR.
US20100022655 Therapeutic Agents For The Treatment Of Lymphoid Malignancies Methods—for treatment and prevention of lymphoid malignancies, including, but not limited to acute lymphoblastic leukemia (ALL), chronic lymphocytic leukemia (CLL), B-cell lymphoma, Acute Myeloid leukemia (AML), and mantle cell lymphoma (MCL). The methods include administration of a therapeutically effective amount of FTY720 (2-Amino-2-[2-(4-octylphenyl)ethyl]propane 1,3-diol hydrochloride) or a derivative, pharmaceutically acceptable salt thereof, or a prodrug thereof to a subject.
WO2005102367A3 Coadministration of radiation, efaproxiral sodium, and supplemental oxygen for the treatment of cancer Disclosed is a method of treating a cancer of the central nervous system in a host including administering radiation to the host; and administering efaproxiral sodium plus supplemental oxygen to the host; wherein the radiation and efaproxiral sodium and supplemental oxygen are administered in amounts effective to cause the arrest or regression of the cancer of the central nervous system in the host.
CN102552358A Silymarin composition and preparation method thereof The invention belongs to the technical field of medicine, which relates to a silymarin composition and a preparation method of the composition. The silymarin composition forms amorphous matter by one or a plurality of silymarin compositions and at least one water-soluble compound. The ratio of the silymarin composition to the water-soluble compound is 10 : (0.5-10); and the water-soluble compound is selected from sugar alcohol, polyethylene glycol, organic acids, surfactant and water-soluble polymers. The dilute solution of the silymarin is dried by using spray drying method or freeze drying method so as to obtain silymarin composition with high solubility and high dissolubility; and the solubility and dissolving-out speed of the silymarin composition are improved.
CN1736421A Main ingredient of anemone rhizome, preparation process and application thereof The invention provides a Diwu extract with a mass content of 60%, which mainly comprises Diwu saponins, the four monomers are, 3-O-beta-D-pyran glucuronic acid-oleanolic acid-28-O-alpha-L-pyran rhamnose(1-4)-beta-D-glucopyranose(1-6)-beta-D-glycopyraniside, 3-O-beta-D-glucopyranose aldehyde acid-oleanolic acid-28-O-beta-D-glucopyranose(1-6)-beta-D-glucopyranoside, 3-O-alpha-L-pyran rhamnose(1-2)-beta-D-glucopyranose-oleanolic acid-28-O-alpha-L-pyran rhamnose(1-4)-beta-D-glucopyranose(1-6)-beta-D-glycopyraniside, 3-O-alpha-L-pyran rhamnose(1-2)-alpha-L-Arabinopyranosyl-oleanolic acid-28-O-alpha-L-pyran rhamnose(1-4)-beta-D-glucopyranose(1-6)-beta-D-glycopyraniside. The invention also discloses the process for preparing the abstract.
EP1538980A1 Devices and methodologies useful in body aesthetics A methodology and system for lysis or induction of apoptosis in cellulite and fat including directing ultrasonic energy at a multiplicity of target volumes within the region, which target volumes contain cellulite and fat, thereby to selectively lyse or induce apoptosis in the cellulite and fat in the target volumes and generally not lyse or not induce apoptosis in non-cellulite and non-fat tissue in the target volumes and computerized tracking of the multiplicity of target volumes notwithstanding movement of the body.
US20110105538 Drug response markers The present invention relates to a method for predicting the response of a disease in a subject, preferably a human, to a drug providing 6-mercaptopurine, the method comprising the step of: (i) determining the presence or absence of a variant allele at a polymorphic site in a human leucocyte antigen (HLA)-G gene wherein the presence of said variant allele at said polymorphic site is indicative of clinical response or tolerance to said drug. The invention also provides a method of treating a subject suffering from a condition that would benefit from a drug providing 6-mercaptopurine.
WO2007146719A3 2-aminocarbonylphenylamino-2-phenylacetamides as factor viia inhibitors useful as anticoagulants The present invention provides novel benzamide derivatives of Formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
US20080269488 Characterized by x-ray reflections at 8.4 degrees, 10.8 degrees, 20.0 degrees, 20.4 degrees, and 21.2 degrees +-0.2 degrees 2 theta. Provided are two novel crystalline forms of gatifloxacin, denominated form O and form V, and methods for their preparation.
CN102100683A Slow-soluble external contraceptive membrane The invention discloses a slow-soluble external contraceptive membrane. The contraceptive membrane is prepared from the raw materials such as 0.05 to 1.5 parts of nonoxinol-9, 0.3 to 2 parts of super carboxymethyl starch sodium, 0.3 to 3 parts of hydroxypropyl methyl cellulose, 0.1 to 0.3 part of polyacrylic resin film agent, 1 to 3 parts of polyethylene glycol, 2 to 10 parts of lubricating agent and the like. The contraceptive membrane prepared by using the material composition has slow solubility and high medicament dissolution, and has effects of absorbing seminal fluid and killing sperms. After the contraceptive membrane prepared from the materials is put into the vagina, sexual intercourse can be performed immediately, and waiting is not needed. The stiff and smooth membrane shape is kept for 3 hours when the contraceptive membrane is not contacted with the seminal fluid, and sperm killing medicaments are slowly released, so that loss of the sperm killing medicaments in short time can be avoided; and the release of the sperm killing medicaments is accelerated when the contraceptive membrane is contacted with the seminal fluid, and the performance ensures high efficiency of the sperm killing medicaments and can improve the contraceptive effect. The membrane material has good compatibility with vaginal mucosa, has irritability resistance, flexibility and comfort, and can eliminate the stimulation effect of the nonoxinol-9 on the skin mucosa.
CN1813776A Medicine for treating pharyngitis and its preparing method The present invention relates to a medicine for curing pharyngitis and its preparation method. It is made up by using bufolactone, liquiritin, citric acid and menthanol through a certain preparation process. Said preparation method includes the following steps: mixing liquiritin, citric acid, menthanol and auxiliary materials of sucrose, saccharin sodium salt, dextrin and microcrystal cellulose, pulverizing them to obtain fine powder, sieving, grinding bufolactone, mixing the ground bufolactone and the above-mentioned medicinal powder, sieving, granulating by using ethyl alcohol, drying, finishing granules, then uniformly mixing them with low-substituted monohydroxypropyl cellulose and magnesium stearate and tabletting so as to obtain the invented product.
CN101439037A Alprostadil lipid complexes and micelle composition thereof for injection The invention belongs to the pharmaceutical preparation field and relates to an alprostadil lipid compound, a micellar compound used in the injection of the alprostadil lipid compound and a preparation method of the alprostadil lipid compound. The alprostadil lipid compound and the micellar compound used in the injection of the alprostadil lipid compound are composed of alprostadil with a therapeutic dose, phospholipid, cholesterol sulfate or/and similar cholesterol derivative, additive and injection water. The alprostadil lipid compound and the micellar compound used in the injection of the alprostadil lipid compound have the advantages of small side effect, low blood vessel simulation, high drug-loading rate, narrow particle size distribution, capability of filtering and degerming, good pharmaceutical stability, etc.
EP1490069B1 Alpha aed and beta aed regulation of nuclear transcription, gene regulation, and/or gene expression The present invention provides a means to regulate nuclear transcription and/or gene expression. The present invention also provides a means to regulate the levels of PPAR-Ϝ, COX-2 and/or NFκB in a patient. The method of the present invention involves administering αAED (or an analogue thereof) or βAED (or an analogue thereof) or both to a patient in need of regulation of nuclear transcription and/or gene expression and/or levels of PPAR-Ϝ, COX-2, and/or NFκB. The methods of the present invention can be used to control adipogenesis (i.e. to treat obesity), angiogenesis, atherosclerosis, mesenteric fat hypertrophy, inflammatory bowel disease, colitis, Alzheimer's disease, and inflammatory glial responses in the brain. The methods of the present invention can also be used for treating diabetes, for regulating the immune response, and for regulating inflammation in a patient.
EP1744774A2 Nutritional composition which promotes weight loss, burns calories, increases thermogenesis, supports energy metabolism and/or suppresses appetite The present invention provides for a nutritional composition including at least garcinia cambogia extract, gymnema sylvestre leaf extract, and green tea leaf extract, consumption of the nutritional composition providing a method of inducing fast weight loss, burning calories, increasing thermogenesis, supports energy metabolism and/or suppressing appetite in individuals. The nutritional composition may be suitable for individuals on a low carbohydrate diet, for individuals on a reduced caffeine or caffeine-free dietary regimen and/or for individuals on a diet of natural ingredients. The present invention may also provide for a method of manufacturing the nutritional composition.
EP2626074A1 Methods and compositions for administration of iron The present invention generally relates to treatment of iron-related conditions with iron carbohydrate complexes. One aspect of the invention is a method of treatment of iron-related conditions with a single unit dosage of at least about 0.6 grams of elemental iron via an iron carbohydrate complex. The method generally employs iron carbohydrate complexes with nearly neutral pH, physiological osmolarity, and stable and non-immunogenic carbohydrate components so as to rapidly administer high single unit doses of iron intravenously to patients in need thereof.
US7151175 Propenecarboxylic acid amidoxime derivatives, a process for the preparation thereof, and pharmaceutical compositions containing the same The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.
WO2013159029A1 Compositions for topical treatment of microbial infections The present invention provides compositions and methods for topical treatment of infections. The compositions comprise glycerol monolaurate or a derivative thereof, and are administered topically, for example, to treat viral, fungal or bacterial infections.
US20120094900 Sensitizing agents for cancer therapy, methods of use and methods for the identification thereof There is provided herein methods, compounds and methods for identifying compounds, for sensitizing a subject with cancer to a cancer therapy by inhibiting or down-regulating UROD.
CN103070842A Preparation method of miglitol sustained release tablet The invention provides a preparation method of a miglitol sustained release tablet. The preparation method comprises the following steps of: I, adding miglitol, Na-montmorillonite and an acidity regulator into deionized water, and stirring uniformly to obtain a mixed solution; II, stirring the mixed solution, performing ion exchange on the miglitol and the Na-montmorillonite, and filtering, washing, drying, smashing and sieving in sequence to obtain a main material; and III, mixing the main material and auxiliary materials uniformly, and tableting to obtain the miglitol sustained release tablet. A preparation process of the method is simple, special equipment and process are not required, and the method is suitable for large-scale batch production. Specific to the defects of the conventional miglitol medicament administration way, a method for compounding the Na-montmorillonite and the miglitol is adopted, so that the in-vivo release rate of the miglitol is lowered, the utilization ratio of a miglitol medicament is increased remarkably, and the taking compliance of a patient is enhanced greatly.
CA2403218C Embolic compositions Embolic compositions comprising macromers having a backbone comprising a polymeric backbone comprising units with a 1,2-diol or 1,3-diol structure, such as polyvinyl alcohol, and pendant chains bearing crosslinkable groups and, optionally, other modifiers. When crosslinked, the macromers form hydrogels having many properties advantageous for use as embolic agents to block and fill lumens and spaces. The embolic compositions can be used as liquid embolic agents and crosslinked in situ or as preformed embolic articles, such as microspheres.
EP2404997A1 Method for enhancing function of t cell Disclosed is a method for enhancing the function of a T cell, which is characterized by inhibiting the expression of programmed death-1 ligand 1 (PD-L1) and/or programmed death-1 ligand 2 (PD-L2) in the T cell. Also disclosed is a function-enhanced T cell which is produced by the function enhancement method. Further disclosed is a therapeutic agent comprising the function-enhanced T cell. The T cell can enhance an immune response to cancer, and is useful in an immunotherapy effective for cancer and the treatment or prevention of infectious diseases and autoimmune diseases.
US20110200583 Asthma Susceptibility Loci Located at Chromosome 1q31 for Use in Diagnostic and Therapeutic Methods Methods and composition are provided for diagnosing pediatπc onset asthma based on the single nucleotide polymorphism on chromosome 1q31 wherein said single nucleotide polymorphism is set forth in Table 2 or Table 6 of the instant invention Method and composition are also provided for treating and preventing asthma or other inflammatory conditions in a patient in need thereof compπsing administering an effective amount of an at least one inhibitor which reduces the expression of DENND1 B gene product.
WO2012053012A2 Topical pharmaceutical compositions comprising tfflocolchicoside The present invention relates to stable pharmaceutical compositions of thiocolchicoside comprising nano size droplets of thiocolchicoside or salts thereof along with other pharmaceutically acceptable excipients. The present invention also relates to stable pharmaceutical compositions of thiocolchicoside comprising nano size droplets of thiocolchicoside or salts thereof, optionally one or more non-steroidal anti-inflammatory agents, along with other pharmaceutically acceptable excipients. These compositions exhibit greater permeability, and improved bioavailability leading to enhanced therapeutic activity. The invention also relates to processes for the preparation of such compositions.
EP1549311A1 Potent inhibitor of hcv serine protease Disclosed are oral pharmaceutical compositions, kits and methods of treating and preventing Hepatitis C Viral (HCV) infections wherein Compound (1), a potent inhibitor of HCV serine protease, or a pharmaceutically acceptable salt thereof, is administered in a selected dosage range: Formula (1) Also disclosed are the use of a compound of formula (1), or a pharmaceutically acceptable salt thereof, as a control substance for validating an HCV replication assay and also as a control substance for determining the relative effectiveness of one or more substances, alone or in combination, to inhibit the replication of HCV.
CN101190936A Compound with antiviral activity The invention pertains to the technical field of medicine, relating to new compounds, which have the activity of antivirus, etc., or stereoisomer thereof, the preparation methods of the compounds or the stereoisomer thereof, medical compositions which comprise the compounds or the stereoisomer thereof as necessary active ingredients, the application of the compounds or the stereoisomer thereof in the preparation of medicine to cure and/or prevent viral infection and hepatopathy. The compounds or the stereoisomer thereof of the invention have the prominent functions of antivirus, in particular to hepatitis B virus and human immunodeficiency virus, and have prominent activity to resist acute and chronic hepatic injury at the same time.
WO2008084873A1 Oxime derivative Disclosed is an oxime derivative represented by the formula below or a pharmacologically acceptable salt thereof, which is a novel compound having an excellent glucokinase activation effect and therefore useful as an active ingredient of a pharmaceutical agent for the prevention and/or treatment of a glucokinase-related disease such as diabetes, diabetic complication or obesity. wherein the ring A represents an aryl group or a heteroaryl group; Q represents a cycloalkyl group, a heterocyclic group or the like; the ring T represents a heteroaryl group or a heterocyclic group; R1 represents a hydrogen atom or the like; R2 represents -COR11 or -CR13(OH)R11; R11 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted cycloalkyl group or the like; R13 represents a hydrogen atom or an alkyl group; R3 and R4 independently represent a hydrogen atom, an alkoxy group or the like; R5 represents a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkyl group or the like; and R6 represents a hydrogen atom or the like.
CN101348482A 3-amido-4-indole maleimide compound, preparation and use thereof The invention discloses a 3-amide-4-indole maleimide and a preparation method thereof. In the structure formula, R is methyl, ethyl, propyl, or the substituted phenyl, wherein the substitutional group can be one or more of the substances including hydrogen, chlorine, bromine, hydroxyl, methoxy or nitryl. The method comprises the following preparation steps that 1) 3-amino-4-(1H-3-indole)-1H- pyrrolidine-2,5-dione and triethylamine are dissolved in solution of tetrahydrofuran, and react with the tetrahydrofuran solution of sulfone chlorideand under the protection by N2, while being mixed under room temperature, after the reaction ends, H2O is added followed by mixing; and 2) the organic layer is extracted with acetic acid, washed with saturated NaHCO3, washed with water, washed with saturated NaCl, dried and condensed with absolute Na2SO4, to obtain the product separated through column chromatography. 3-amide-4-indole maleimide is a novel inhibitor of protein kinase C, and can be applied to preparation of drugs for treatment and prevention of tumor, diabetes, and complications of diabetes.
US7105670 Intermediates useful in the preparation of diaminothiazoles Disclosed are novel diaminothiazoles that are selective inhibitors of Cdk4. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds as well as intermediates useful in the preparation of the compounds.
WO2008049806A1 Piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid mtp inhibiting compounds The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
WO2009024611A3 4-benzylaminoquinolines, pharmaceutical compositions containing them and their use The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors.
WO2008046049A1 Spiro (furo [3, 2-c] pyridine-3-3 ' -indol) -2' (1'h)-one derivatives and related compounds for the treatment of sodium-channel mediated diseases, such as pain This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein j, k, m, Q, X,, R1, R2a, R2b, R2c, R2d and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, N-oxide, solvate or prodrug thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
CN1593438A Aseptic diammonium glycyrrhizinate powder injection and its preparation The invention discloses an aseptic diammonium glycyrrhizinate powder injection and its preparation, wherein the preparation consists of, under asepsis condition, dissolving the diammonium glycyrrhizinate raw material with ethanol, adjusting pH to be 7.0-8.0, removing impurity by charging activated carbon, processing the soup with degerming filtration, dispensing the filtered soup for recrystallization, drying and split charging.
CN102008437B Rapamycin microemulsion injection for eyes and preparation method and application thereof The invention discloses rapamycin microemulsion injection for eyes and a preparation method and application thereof. In the injection, rapamycin is taken as an active ingredient and is added with a pharmaceutically acceptable carrier, and each 1,000ml of preparation contains 0.05 to 20g of rapamycin. The microemulsion injection for eyes has low cost and high stability, does not have obvious irritation and toxic or side effect on the eyes, can be used for treating retinal degenerative diseases, and particularly has obvious effect of treating age-related macular degeneration disease. The treatment effect of the injection is provided on the basis of breakthrough and discovery of a pathogenic mechanism, and the rapamycin microemulsion injection has profound significance for treating the diseases.
EP1307182B1 Pharmaceutical composition for transdermal delivery of befloxatone The invention concerns a pharmaceutical composition for transdermal delivery of befloxatone, capable of being in the form of gel, ointment or transdermal patch or a sprayed film. The invention is characterised in that it comprises at least an absorption promoter.
US7098202 Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
US20120309762 Cytochrome p450 oxidase inhibitors and uses thereof The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.
WO2006099681A1 Isoflavonoid dimers Novel compounds based on phenyl-substituted naphtho[l,2-g]chrysene compounds (A) are described. The compounds are obtainable by dimerisation of 3-phenylchroman (isoflavonoid) ring systems (B). Methods of synthesis of the novel dimeric compounds, compositions containing same and use of the dimers as therapeutic agents are also described.
CN102757555A Dequalinium chloride-polyethylene glycol-distearoyl phosphatidyl ethanolamine conjugated compound and resveratrol liposome modified thereby The invention discloses a DQA-PEG 2000-DSPE (Dequalinium Chloride-Polyethylene Glycol-Distearoyl Phosphatidyl Ethanolamine) conjugated compound and resveratrol liposome modified thereby. The structural formula of the compound is shown by a formula I. In terms of composition, the resveratrol liposome comprises resveratrol and a fat material, wherein the mass ratio of the resveratrol to the fat material is (1:20)-(1:40); and the fat material consists of egg yolk lecithin, cholesterol and the compound shown by the formula I in the molar ratio of (63-67):(18-22):(2-4.35) in sequence. Pharmacodynamic tests prove that mitochondrial targeted resveratrol liposome has an extremely strong cell toxic effect in in-vitro cell experiments of human lung adenocarcinoma A549 cells and drug-resistant A549/cDDP cells thereof, a tumor sphere model and an in-vivo transplantation tumor model and can penetrate through the core of the tumor sphere. The anti-tumor effect of vinorelbine liposome on the drug-resistant A549/cDDP cells can be obviously improved by combining the resveratrol liposome with the vinorelbine liposome for use (formula I).
EP1798225A1 Nucleoside analogues or salts thereof It is an object to provide a nucleoside analog that can produce an oligonucleotide analog in which the two properties of chemical and biological stability, and the ability to form double strands, are excellent, and an oligonucleotide analog that includes that nucleoside analog. This is achieved by a nucleoside analog or salt thereof represented by Formula (1) below, in which, in Formula (1), R1 is any group selected from the group consisting of the group of Formula (1), the group of Formula (2), the group of Formula (3), the group of Formula (4), the group of Formula (5), the group of Formula (6), the group of Formula (7), the group of Formula (8), and any of these groups whose functional group has been protected by a protecting group, and k, l, m, and n are each independently an integer from 1 to 10.
US20120010223 Isothiazolo-pyrimidinedione derivatives as trpai modulators The present invention is related to novel isothiazolo[3,4-d]pyrimidinedione and isothiazolo[5,4-d]pyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
EP1499206A1 Hydrothermically processed compositions containing phytosterols Hydrothermically formed phytosterol-emulsifier compositions are disclosed, along with the process for their production. The compositions are organoleptically pleasing and useful in foods, health products, and nutraceutical products for lowering cholesterol levels. Phytosterols are mixed with an emulsifier dispersion and then hydrothermically heated to integrate the phytosterols into a micellar form with the emulsifier, which produces a smooth and pleasing mouthfeel and a bioactive and bioavailable product.
CN102488882A Compound propolis composition for treating porcine respiratory disease syndrome and preparation method thereof A compound propolis composition for treating porcine respiratory disease syndrome and a preparation method thereof relate to the field of animal medicine. The composition of the invention is prepared by the following method: (1) carrying out ultramicro crushing respectively on various components (except an interferon) in the composition and sieving through a 700 mesh screen; (2) weighing 15-35 parts of propolis, 15-30 parts of tussilago, 10-35 parts of the bulb of fritillary, 15-40 parts of balloonflower root, 10-40 parts of anemarrhena and 10-35 parts of bitter apricot kernel; (3) weighing 10-35 parts of radix ophiopogonis, 15-45 parts of cape jasmine, 15-25 parts of licorice, 15-55 parts of gypsum, 15-35 parts of Chinese holly and 15-45 parts of ginger and mixing 5-10 min to a uniform state; and (4) merging the combinations prepared in the steps (2) and (3) and mixing 10-15 min to a uniform state. The invention has beneficial effects of reasonable composition and simple preparation; the composition has no toxic or side effect, pollution, medicament residual or drug resistance, and is processed by ultramicro crushing to realize a high bioavailability; and the composition has substantial curative effect and special efficacy on porcine respiratory disease syndrome according to clinic proving.
US20080300273 Method of Treating Abnormal Cell Growth The present invention relates to the use of (R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, a novel c-Met/HGFR inhibitor, for treating abnormal cell growth in mammals. In particular, the invention provides methods of treating mammals suffering from cancer.
CN102920683A Olanzapine oral instant membrane The present invention belongs to the field of pharmaceutical preparations, particularly relates to an olanzapine oral instant membrane agent, a preparation method and pharmaceutical uses thereof. The membrane agent comprises the following components, by weight, 1-30% of olanzapine, 40-90% of a polymer membrane forming material, 0-40% of a plasticizer, 0-30% of a flavoring agent, and 0-5% of otherauxiliary agents. The olanzapine oral instant membrane agent has the following characteristics that: no water is required during administration, the olanzapine oral instant membrane agent can rapidlymelt in mouth, phenomena of drug hiding in mouth and drug spitting of schizophrenia patients can be avoided, and patient medication compliance is easily improved. With the preparation method, the main drug of the olanzapine oral instant membrane agent has characteristics of good dispersing effect in a hydrophilic matrix glue liquid, good finished product appearance, rapid dissolution and good stability. In addition, characteristics of accurate product dose and no dust flying during a production process are provided, and problems of labor protection and environmental pollution can be solved.
US20110046136 Methods for the production of functional protein from dna having a nonsense mutation and the treatment of disorders associcated therewith The present invention relates to functional proteins encoded by nucleic acid sequences comprising a nonsense mutation. The present invention also relates to methods for the production of functional proteins encoded by nucleic acid sequences comprising a nonsense mutation and the use of such proteins for prevention, management and/or treatment of diseases associated with a nonsense mutation(s) in a gene.
US20130280303 Bone delivery system having a therapeutic agent A covering for delivering a therapeutic agent to a surgical site is provided. The covering may include a single or multi-compartment structure configured to at least partially retain the therapeutic agent until the covering is placed at a surgical site. Upon placement, the covering may facilitate transfer of the therapeutic agent to the surgical site. In some embodiments, the covering comprises an antimicrobial agent, a hemostatic agent, an anti-inflammatory agent, and/or a growth factor.
WO2009010925A3 Annelated azaheterocyclic amides containing a pyrimidine fragment and method for the production and use thereof The invention relates to novel annelated azaheterocycles of general formula 1, containing a pyrimidine fragment in the form of free bases or pharmaceutically acceptable salts, to pharmaceutical compositions containing said compounds and to the use of said compounds for producing medicinal preparations and therapeutic cocktails for treating human and homothermal diseases caused by a class I phosphoinositol kinase (PI3Ks) activity (and mutant isoforms thereof), in particular oncological diseases, to the use of said compounds as 'molecular pharmacological instruments' for studying (in vitro and in vivo) biochemical mechanisms of (PI3Ks) kinase action, in particular class I kinases (PI3Ks) and mutant isoforms thereof. In the formula 1, X is an oxygen atom,a sulphur atom or an optionally nitrogen-substituted group; Y is a nitrogen atom or an optionally carbon-substituted CH group; Z is an oxygen atom; R1 is a hydrogen atom or optionally substituted C1-C6 alkyl or Z is a nitrogen atom which, together with an carbon atom, to which it is bound, form, via Z and R1, an optionally substituted imidazoline cycle; R2 and R3, independently from each other, are optionally substituted alkyl, optionally substituted aryl or heterocycle, wherein Y is an optionally carbon-substituted CH group, X=O,S, or R2 is hydrogen, R3 is substituted aminoalkyl or optionally substituted azaheterocyclyl alkyl, wherein optionally substituted azaheterocyclyl alkyl or R2 is hydrogen, R3 is substituted aminoalkyl or optionally substituted azaheterocyclyl alkyl, R1 is substituted aminoalkyl, substituted hydroxy alkyl or optionally substituted azaheterocyclyl alkyl, Y is an optionally carbon-substituted CH group, X=O,S; R4 is hydrogen or lower alkyl.
WO2010016042A8 Treatment of retinal degeneration The use of a compound having a gon-4-ene nucleus, said nucleus having attached thereto, in the 13 position, a polycarbon-alkyl radical having 2 to about 16 carbon atoms, said compound containing at least 19 and up to 40 carbon atoms in its carbon-carbon skeleton, in the manufacture of a medicament for the treatment or prevention of a disease or condition characterised by apoptosis or degeneration of mammalian cells.
CN102863345A Amino propylene glycol derivative, preparation method of amino propylene glycol derivative, medicine composition of amino propylene glycol derivative and application of amino propylene glycol derivative The invention provides an amino propylene glycol derivative, a preparation method of the amino propylene glycol derivative, a medicine composition of the amino propylene glycol derivative and application of the amino propylene glycol derivative. The invention discloses an immunomodulator shown as a general formula (I), a preparation method of the immunomodulator, a medicine composition containing the immunomodulator, and application of the immunomodulator serving as a medicine, particularly the application serving as an immunomodulatory medicine. The compound which is excellent in curative effect and low in toxicity can be used for aspects of immunologic derangement and immunosuppression, and can be used for treating hypoimmunity, rejection reaction after organ grafting and/or autoimmunity diseases.
CN101396344A Paeonol microemulsion preparation and preparation method thereof The invention relates to the medical technical field, in particular to a paeonol micro-emulsion preparation and a preparation method thereof. The paeonol micro-emulsion preparation consists of components with the weight percentage as follows: 0.1 percent to 2 percent of paeonol, 10 percent to 25 percent of surfactant, 5 percent to 30 percent of cosurfactant, 5 percent to 15 percent of oil phase and 40 percent to 70 percent of deionized water. The mouse percutaneous experiment in vitro shows that the paeonol micro-emulsion prepared by the invention has obviously higher capacity of penetrating through the horny layer than the saturated aqueous solution of paeonol (p is less than 0.05), and the paeonol micro-emulsion can penetrate into the skin deeply to take curative effect within a short time and also has certain sustained and controlled release function. At the same time, the paeonol micro-emulsion improves the solubility of the paeonol obviously, increases the drug loading quantity of the preparation and reduces the drug administration times and the dosage. The paeonol micro-emulsion preparation has simple preparation method and uniform grain diameter of the preparation, has the advantages of being safe, stable and efficient and, can be used for preparing dermal medication preparation or cosmetic.
US20110313229 Therapy Targeting Cancer Stem Cells Disclosed herein are new immunotherapy methods that involve the isolation of cancer stem cells from tumor tissue and use of the cells either directly or indirectly through proteins or other factors associated with the cells to activate antigen presenting cells. The activated antigen presenting cells are useful as a therapy against the tumor. Also disclosed herein are novel methods of isolating and characterizing cancer stem cells and producing individual cancer stem cell lines. Dendritic cell lines are also disclosed herein.
WO2007028903A1 Novel combination between agomelatine and a thymoregulating agent and pharmaceutical compositions containing same The invention concerns a combination between agomelatine or N-[2-(7-methoxy-1-naphtyl)ethyl]acetamide in association with a thymoregulating agent for treating mood disorders.
CN1720999A Hab18G/CD147 molecule small segment interfering RNA medicine and application thereof Disclosed is a Hab18G/CD147 molecule small segment interfering RNA medicine for resisting tumor mesenchyma degradation and antiphlogistic infection, which uses liver cancerometastasis correlation coefficient Hab18G/CD147 as targeting target molecules for designing and synthesizing small fragment interference RNA depressant, its functions include blocking-up effect cells (desmocyte, synovial membrane cells) induced secretion of metalloproteinase (MMPs), diminishing tumor tissue mesenchyme degradation and formation of articular cartilage encroachment and pannus, thus can achieve the goals of treating recurrence and transfer of tumors including liver cancer, rheumatoid arthritis and osteoarthritis.
CN101569603B Doxofylline-contained liquid injection, preparation method thereof The invention relates to a doxofylline-containing liquid injection used for treating bronchiectasis, and provides the doxofylline with higher concentration. The injection comprises doxofylline, a water solvent, and a pH value regulating agent. The injection comprises the following components by weight percentage: 1 to 4 percent of the doxofylline, and 0.01 to 5 percent of the pH value regulating agent. The injection enriches specifications of the prior doxofylline injection, and brings convenience to the clinical application. The invention also provides a preparation method and a quality control method for the doxofylline liquid injection. Relevant materials in the doxofylline injection can be determined by an HPLC method to improve the product controllability.
WO2007024294A3 Certain substituted ureas, as modulators of kinase activity Certain chemical entities chosen from compounds of Formula (1) and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
US20070231405 Compositions and Methods Using Same for Treating Neurodegenerative Disorders Compositions and methods of using same are provided for the treatment of neurodegenerative disorders such as Glaucoma, Multiple Sclerosis, Myasthenia Gravis, Diabetic Neuropathy, Cerebrovascular accident, spinal cord injuries, ALS, Parkinson's disease and Idiopathic dementia.
US20100173907 Method of treatment of aggression The invention comprises a method of treatment of aggression and similar behavioral syndromes, such as impulsivity and irritability, by a pharmaceutical agent exhibiting combined D2 and D5 antagonistic activity.
US20090155193 Topical Bioadhesive Formulations The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
WO2013192352A1 Antibacterial agents: aryl myxopyronin derivatives The invention provides compounds of formula la, lb and Ic: [Formula Ia, Ib, and Ic] and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula Ia-Ic, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.
EP1832592A2 15-C Isomers of rapamycin and of 42-EPI rapamycin, preparation and use thereof 15-C isomers of rapamycin and of 42-C Epi rapamycin, and pharmaceutically acceptable salts or prodrugs thereof are disclosed. These compounds are potential immunomodulatory and anti-inflammatory agents, and may be useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post- transplant tissue rejection- and immune- and autoimmune disease- inhibiting compositions comprising the invented isomers, and methods of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of these novel rapamycin derivatives are in implantable medicated devices wherein the prolonged presence of these compound locally are essential to the success of drug containing combination devices.
US6946489 Substituted biphenyl derivatives The invention relates to compounds of the formula I in which R1, R2, R3, R4 and X have the meaning indicated in the text. The compounds act as inhibitors of factors Xa and VIIa and can therefore be employed for the control and prevention of thromboembolic conditions such as thrombosis, myocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.
EP2698159A1 Pitavastatin-containing preparation and method for producing same The present invention provides: a pitavastatin-containing preparation, which is characterized by containing pitavastatin or a pharmacologically acceptable salt thereof and at least one basic additive selected from the group consisting of basic magnesium compounds and basic calcium compounds, and which is also characterized in that an aqueous solution or aqueous dispersion thereof has a pH of more than 8 but 10 or less; and a method for producing a pitavastatin-containing preparation, which is characterized in that the above-described specific basic additive is blended with pitavastatin or a pharmacologically acceptable salt thereof so that an aqueous solution or aqueous dispersion thereof has a pH of more than 8 but 10 or less.
CN102973701A Drug for treating dermatophytosis, and preparation method thereof The invention relates to a drug for treating dermatophytosis. The drug is composed of radix sophorae flavescentis, herba schizonepetae, coptidis rhizome, cortex phellodendri, borneol, sandalwood, gypsum, cnidium monnieri, etc. Compared with a conventional drug for treating dermatophytosis, the drug provided by the invention has the advantages of dispelling dampness, relieving itching, removing fungus, uneasy recurrence and the like, and can be widely applied in life.
US20120077823 Controlled release systems of pluribioactive antifungal drugs and applications thereof Controlled release systems release at least one pluribioactive antifungal drug exhibiting at least one additional bioactivity from the group consisting of spermiostatic, antineoplastic, antibacterial, antirestenotic and antiviral activities. The drug release system is designed for use as a spermiostatic contraceptive, intravaginal ringed-mesh which may also exhibit antiviral activity, an in situ-forming implant for treating different forms of cancer and topical film for treating or preventing bacterial and fungal infections.
US20100303819 Dcl-1 and uses thereof The present invention relates generally to a novel lectin and to derivatives, homologues, analogues, chemical equivalents and mimetics thereof and, more particularly, to a novel type I C-type lectin, herein referred to as “DCL-1”. In particular, the present invention relates to the use of DCL-1 in therapeutic, prophylactic and diagnostic applications.
US6900161 Azole or triazole derivatives, method for preparing same and use thereof as fungicides The invention concerns novel azole or triazole derivatives of formula (Ia) or (Ib), wherein: X, Ar1, Ar2, Ar3, A, B and R1 are such as defined in the description, the method for preparing same and their use as fungicides.
CN101596162B Doxycycline hyclate enteric-coated pellet The invention discloses a doxycycline hyclate enteric-coated pellet which comprises the following components in percentage by weight from inside to outside: 48-58 blank core pellet, 35-40 medicinal layer and 4-13 enteric-coated layer. The invention also discloses a method for preparing the doxycycline hyclate enteric-coated pellet. The doxycycline hyclate enteric-coated pellets prepared by the method are filled into a capsule, and an obtained enteric-coated preparation has the advantages of increased contact area with the intestinal tract, high bioavailability, good stability, steady release in vitro and vivo, no influence by gastrointestinal peristalsis and food intake, uniform absorption, smaller difference of bioavailability among individuals, and the like.
US20080064680 Methods for Diagnosis and Treatment of Cancer The present application discloses methods of detecting and treating cancer which express MUC1 aberrantly.
WO2009100011A2 Targeted cellular selectivity of surface active molecules A method for the treatment of cancer involves delivering a surface active agent to an organism, where the surface active agent selectively partitions to and kills cancer cells as opposed to healthy cells. The surface active agent can be an ionic or a non-ionic surfactant with a HLB of less than 29 or a mixture of surface active agents with a HLB of less than 40, where the hydrophobic portion is a lesser fraction of the surface active agent than the hydrophilic portion. A fluorescence method of detecting and locating cancer cells in an organism involves delivering a surface active agent, where the surface active agent includes a fluorescence moiety that upon selective partitioning of the surface active agent to the cancer cells and irradiation by a radiation source to excite the fluorescence moiety, a fluorescence emission is observed permitting the detection and location of the cancerous tissue by local volumes of relatively high intensity emission.
CN102805744A Pharmaceutical composition for treating or preventing obesity and metabolic syndrome The invention discloses pharmaceutical composition for treating or preventing obesity and metabolic syndrome and belongs to the field of pharmaceuticals. The pharmaceutical composition comprises active ingredients, namely orlistat and miglitol according to a preferable weight ratio of 1:0.1-100, and a more preferable weight ratio of 1:0.5-10. The pharmaceutical composition can be made into conventional pharmaceutical dosage forms, preferably the solid form. The pharmaceutical composition has evident synergistic effect on treating or preventing obesity and metabolic syndrome, is capable of lowering the risks of cardiovascular diseases and has broad medical application prospect.
US6949579 Central nervous system disorders; antidiabetic agents The present invention relates to the novel indazole derivatives of general formula (I): in which: R is either O, S or NH; R3 is an alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryl, heterocycle, cycloalkyl, alkenyl, etc. radical; these radicals being optionally substituted with one or more substituents; R4, R5, R6 and R7 are chosen, independently of each other, from the following radicals: hydrogen, halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycle, cycloalkyl, alkenyl, etc.; these radicals being optionally substituted with one or more substituents.
WO2005118612A1 Cholesterol/bile acid/bile acid derivative-modified therapeutic anti-cancer drugs Cholesterol-modified anti-cancer therapeutic drug compounds, bile-acid-modified anti-cancer therapeutic drug compounds, and bile-acid-derivative-modified anti-cancer therapeutic drug compounds; emulsion, microemulsion, and micelle formulations that include the compounds, methods for administering the compounds and formulations; and methods for treating cancer using the compounds and formulations.
EP1255749B1 Tyrosine derivatives with anti-leukotriene activity Compounds which can be represented by general formula (I) useful in treatment of pathological conditions sentive to leukotriene inhibition.
EP1658848A1 Formulations comprising ecteinascidin and a disaccharide Ecteinascidin formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided.
EP1499594A1 Process for the preparation of 7-substituted-3-quinoline and 3-quinol-4-one carbonitriles There is provided a process for the preparation of 7-substituted-3-quinolinecarbonitriles and intermediates useful in a process to prepare 7-substituted-3-quinolinecarbonitriles and pharmaceutically acceptable salts is described. Where 7-fluoro-4-oxo-1,4-dihydro-3-quinolinecarbonitrile is converted in three steps to 7-substituted-3-quinolinecarbonitriles which inhibit the action of certain protein kinases and are useful in the treatment of cancer.
CA2558629A1 Trihemihydrate, anhydrate and hydrate forms of cefdinir The present invention relates to trihemihydrate, novel lower hydrate and anhydrate forms of 7-[2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamide]-3-vinyl-3-cephem-4-carboxylic acid (syn isomer), methods for their preparation, and pharmaceutical compositions comprising these forms.
EP1336612B1 Novel carbapenem derivatives It is intended to provide carbapenem derivatives which have a potent antibacterial power on MRSA, PRSP, Haemophilus influenzaeand β-lactamase-producing bacteria and a high stability to DHP-1. The above compounds involve compounds represented by the following general formulae (I) and (II) and pharmaceutically acceptable salts thereof, wherein R1 represents H or methyl; R?2 and R3¿ represent each H, halogeno, optionally substituted alkyl, cycloalkyl, optionally substituted alkylcarbonyl, carbamoyl, optionally substituted aryl, optionally substituted alkylthio, morpholinyl, alkylsulfonyl or formyl; n is from 0 to 4; and Hy represents an optionally substituted, monocyclic or bicyclic heterocyclic group.
WO2007137808A1 Compositions comprising oligosaccharides for treating prion disease The present invention provides the use of a substituted or unsubstituted linear, branched or cyclic oligosaccharide comprising from 2 to 10 monosaccharide units, for the preparation of a medicament for treating prion disease. The present invention also provides a pharmaceutical composition for treating prion disease, the composition comprising a pharmaceutically effective amount of a substituted or unsubstituted linear, branched or cyclic oligosaccharide comprising from 2 to 10 monosaccharide units, with the exception of unsubstituted β-cyclodextrin, and a pharmaceutically acceptable excipient.
CN101167720B Application of iridoids compound in preparing medicine for treating benign prostate hyperplasia The invention discloses the usage of iridoid compounds in preparing the drug for the treatment of benign prostatic phyperplasia. The compounds come from valerianaceae plants which have a long medical history and excellent safety. The drug-effect substance of the compounds is clearer than original spider fragrant plant extract. The invention makes the possibility for good market outlook of new anti benign prostatic phyperplasia medicament.
US6881548 Methods and kits for diagnosing tumorigenicity and determining resistance to the antineoplastic effects of antiestrogen therapy Methods and kits for diagnosing tumorigenicity and for determining whether a cancer patient is resistant to the pharmacological effects of antiestrogen therapy. Increased levels of the PCDGF (GP88) growth factor are indicative of tumorigenicity and resistance to the pharmacological effects of antiestrogen therapy. The methods and kits of the invention are useful for assessing the tumorigencity of a biological sample from a patient and determining whether the patient is a candidate for antiestrogen, including tamoxifen, therapy.
CN101103997A Colored medicinal charcoal film coated tablet preparation method The invention discloses a preparation method of painted medicinal carbon film-coating tablet produced by the raw material of medicinal carbon and medicinal excipients. The invention is characterized in that painted medicinal carbon film coating tablets are produced in the preparation method, thus the visual defect of black medicinal carbon is overcome and the painted tablets are easy to be accepted by patients. The smooth and round form of the painted medicinal carbon film coating tablet can help effectively guarantee the tablet quality and improve the clinical compliance of patients.
CN102846589A Long term weight maintenance This invention is in the field of weight maintenance, more in particular in the field of long term weight maintenance of humans. The invention relates to the use of a mixture of a triglyceride oil having a solid fat content at ambient to body temperature and an emulsifier for maintaining weight after weight loss. The invention also relates to the use of a mixture of a triglyceride oil having a solid fat content at ambient to body temperature and an emulsifier for obtaining a thermogenic effect. The invention also relates to the use of a mixture of a triglyceride oil having a solid fat content at ambient to body temperature and an emulsifier for increasing the energy expenditure such as resting energy expenditure.
CN101125141A Anticancer medicine composition and its application in preparing anticancer medicine The present invention discloses an anti-cancer pharmaceutical composition and the application in the preparation of colorectal cancer drugs, the application in the preparation of breast cancer drugs and the application in the preparation of lung cancer drugs. The pharmaceutical composition of the present invention includes the raw materials with the following weight percentages: 0.1 to 5 parts of 1-hydroxy-britannilactone, 0.1 to 5 parts of 1-oxygen-acetylbritannilactone and 0.1 to 5 parts of 1, 6-dioxygen-diacetylbritannilactone. The pharmaceutical composition of the present invention has significant anti-cancer activity, less toxicity and fewer side effects. At the same time, the pharmaceutical composition of the present invention is the active ingredient, which can be prepared into various pharmaceutical preparations, so the present invention can provide a new drug option for the clinical treatment of various cancers. The present invention particularly provides the new option for the treatment of colorectal cancer, breast cancer and lung cancer.
US20050171118 Central nervous system, gastrointestinal and psycological disorders; such as 3-(4-chlorobenzenesulfonyl)-2-methyl-7-piperazin-1-yl-1H-indole; synthesis This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein one of R5, R6 or R7 is a group of general Formula B, wherein W is a —CH— group or a nitrogen atom, and the other substituents are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
CN1903201A Injection prepn. contg. 10-hydroxy-9-allyl-camptothecine, and its prepn. method An injection of 10-hydroxy-9-ally camptothecine is prepared from 10-hydroxy-9-ally camptothecine, non-ionic surfactant as solubilizer, and cosolvent chosen from alcohol, propanediol, propanetriol and polyethanediol. Its preparing process is also disclosed.
US20090253778 DNA composition against tumor stromal antigen FAP and methods of use thereof A DNA composition effective for eliciting an immune response against tumor cells and tumor metastases comprising a DNA construct that encodes for at least one epitope of fibroblast activation protein (FAP), which is expressible in immune cells, and which is incorporated in a pharmaceutically acceptable carrier. The composition can encode a single epitope of FAP, a polypeptide comprising two or more epitopes of FAP, the entire FAP protein, or any portion thereof that will elicit the desired immune response. In one preferred embodiment, the composition also includes a DNA construct that encodes an immune effector protein, such as a cytokine. The DNA composition of the invention can be used alone or in combination with a chemotherapeutic agent to treat diseases such as tumors and tumor metastases.
US7001899 7-member ring N-heterocycles that have a cysteine trap substitution; treating osteoarthritis The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: wherein each X is independently selected from: i) —C(W)2—; ii) —C(O)—; iii) —NR2—; iv) —S—; v) —S(O)—; vi) —S(O)2—; vii) two units, one from each adjacent X unit, can be taken together to form a substituted or unsubstituted double bond having the formula —CW═CW—; wherein each W is hydrogen of a unit having the formula —(L2)j—R2, the index j is 0 or 1; R is a carbocyclic or heterocyclic aryl ring; R1 is a cysteine trap; each R2 is independently a suitable substituent; and L, L1, and L2 are linking units.
CN101961343A Injection ribonucleic acid and production method thereof The invention discloses injection ribonucleic acid. The injection ribonucleic acid is characterized in that every 1,000 injections contain 10.0g of ribonucleic acid, 30.0g of dextran, 40.0g of mannitol, 9.0g of sodium chloride, 1.0g of medicinal carbon and 1,000ml of fresh injection water. A production method of the injection ribonucleic acid comprises the following steps of: arranging bottles; washing, baking and sterilizing bottles; washing, baking and sterilizing plugs; preparing; filling; performing freeze drying; capping; performing lamp inspection; packaging; and warehousing. The process flow is simple, the preparation operation time is shortened, the production process can be controlled within a specified time limit range, and the method is more suitable for batch production in workshops; after the process is changed, the qualification rate of the freeze-drying of the product is improved by 4 percent; after the level of the production process of the injection ribonucleic acid is increased, the product property is stable, and all the items to be inspected meet the specifications; and the yield of the raw materials is correspondingly improved, the production cost is reduced, and the market competitiveness of the product is improved.
US20100203107 Methods of Administering a Dermatological Agent to a Subject Methods for administering a dermatological agent to a subject are provided. In the subject methods an effective amount of a topical formulation of the dermatological agent is topically applied to a host. The topically applied formulation of dermatological agent is then occluded with a hydrogel patch, where a feature of the hydrogel patch is that it lacks a pharmaceutically active agent. Also provided are methods of treating a subject for a disease condition by administering a dermatological agent to the subject. Also provided are kits for use in practicing the subject methods. The subject methods and compositions find use in a variety of different applications.
CN101116663A Percutaneously absorbable preparation for treating male sexual disfunction and method for preparing the same The invention discloses a percutaneous absorption preparation for curing male sexual dysfunction and the preparation method thereof. Calculated on the basis of total weight of the preparation, the composition at least contains 2.5 percent to 5 percent phentolamine mesylate and 2.5 percent to 5 percent papaverine hydrochloride or papaverine. The preparation adopts percutaneous administration method and completes administration through penis and scrotum skin to make phentolamine mesylate, papaverine hydrochloride or papaverine directly act on penis artery and smooth muscle so as to strengthen erection of penis, thereby being capable of effectively curing male sexual dysfunction; meanwhile, the invention avoids toxic and side effects caused by the prior cavernosum injection and oral taking medicinal preparation and is convenient in use, thereby has ideal compliance of patient.
WO2009026701A1 Sirtuin inhibitors This invention relates to compounds and methods for the inhibition of sirtuin enzymatic activity. More particularly, the invention provides for compounds of formula (I), Y__L__Z__D, and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein Y, L, Z and D are as defined in the specification.
EP2011501A1 Compounds with chelation affinity and selectivity for first transition series elements and their use This invention involves the use of a class of compounds with chelation affinity and selectivity for first transition series elements. Application or administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease of the bioavailability and/or chemical action of first transition series elements. These characteristics make such compounds useful in cosmetics and personal care products to decrease odor arising from microbial growth on body surfaces and in body cavities, decrease microbial growth on teeth, plaque, and gums that cause tooth decay and gum disease, inhibition of oxidative damage to the skin, inhibition of enzymatic action of metalloenzymes dependent on first transition series elements, and inhibition of reperfusion injury.
WO2013051435A1 Therapeutic agent, gene therapy agent, and method for preventing invasion of eosinophil [Problem] To provide: a therapeutic agent for eosinophilic sinusitis and eosinophilic otitis media; a gene therapy agent; and a method for preventing the invasion of an eosinophil. [Solution] A therapeutic agent which can be used for the treatment of eosinophilic sinusitis and/or eosinophilic otitis media, which comprises siRNA capable of inhibiting the expression of a STAT-6 gene, siRNA capable of inhibiting the expression of a GATA-3 gene and/or siRNA capable of inhibiting the expression of an IL-5 gene as an active ingredient.
EP1930011A2 Crystalline form of ibandronate sodium The present invention relates to a crystalline form of ibandronate sodium characterised by x-ray reflections at about 6.2, 15.7, 26.3, 32.6 and 35.6 ± 0.2° 2θ with further x-ray reflections at about 17.6, 19.4, 26.9, 31.7 and 38.7 ± 0.2° 2θ. The x-ray powder diffraction diagram is shown in the figure. Pharmaceutical compositions comprising said crystalline ibandronate sodium are also claimed.
CN102000114A Injection egg white pig fattening agent and preparation method thereof The invention aims to provide an injection egg white pig fattening agent and a preparation method thereof, belonging to the technical field of pig raising methods and relating to a drug which is beneficial to development and rapid fattening of a pig. The preparation method mainly comprises the following steps of: carrying out dilution preparation on ten mineral substances like egg white, copper, ferrum, zinc, manganese, calcium, phosphorus, sodium, magnesium, selenium and the like by using distilled water and a glucose solution to form a prepared solution and preparing an injection (10ml per one) by using the prepared solution. The injection fattening is carried out on healthy pigs of 40-50kg. The injection site of the pig is 1-5cm site at the turning of mandible permanent tooth germ abutted with the bone margin site, and a needle head faces the direction of the head and forms an angle of 35-60 degrees with the neck. The invention has the advantages of not having toxic and side effects and taking the complementation and promotion action on development fattening and feed nutrition of the pig. After the pig fattening agent is injected at a time, the appetite of the pig is obviously enhanced and the growing speed is high. The pig fattening agent also takes the obvious effect on enhancing the immunological effect. The invention has the mechanism that through injecting the pig fattening agent to the site approaching the pituitary and the hypothalamus of the pig, the endocrine functions of the pituitary and the hypothalamus of the pig are promoted, and then the pig fatting is emphasized.
CN103638016A Application of Manzamenone O in rectal cancer treatment drugs The invention discloses an application of Manzamenone O in rectal cancer treatment drugs, belonging to the technical field of new application of drugs. According to in-vitro MTT antitumor activity evaluation, the Manzamenone O has a remarkable inhibitory effect on the growth of human rectal cancer cell strains LOVE1, LOVO, SW620 and SW480. Therefore, the Manzamenone O can be used for preparing anti-rectal cancer drugs and has a good prospect in development and application. The application of Manzamenone O in preparation of rectal cancer treatment drugs is disclosed for the first time; the Manzamenone O has strong inhibitory activity on the rectal cancer cells, and a remarkable progress is realized.
WO2008110491A3 Chemotherapy of neoplastic diseases using combinations of rapamycin and compounds modulating mtor pathway alone or in combination with heat The invention relates to compounds blocking or activating the mTOR pathway for use as a medicament in combination with rapamycin or a rapamycin-like compound and/or with metformin or a metformin-like compound and/or with thermal energy, for the treatment of neoplastic diseases, hyperproliferative conditions or other processes wherein mTOR is implicated. Experiments are described which demonstrate that mutational loss of Tsc2 or PTEN or down-regulating Tsc2 or PTEN by shRNA sensitizes cells for rapamycin and metformin and for thermal treatment, with synergies of these three forms of treatments. The invention further relates to a method to predict sensitivity of a tumor to the combination of mTOR pathway inhibition combined with application of thermal energy.
US20070021333 Pharmaceutical compositions based on anticholinergics and soluble tnf receptor fusion proteins The present invention relates to novel pharmaceutical compositions based on anticholinergics and soluble TNF receptor fusion proteins, processes for preparing them and their use in the treatment of respiratory diseases.
EP2007385A2 Cardiovascular composition and use the same for the treatment of alzheimers disease Methods and compositions for the treatment of Alzheimer's Disease are described. More specifically, the invention demonstrates that administration of cardiovascular agents to a mammal suffering from the symptoms of Alzheimer's Disease causes an amelioration of those symptoms. The finding of the present invention can be used in treatment regimens designed to attenuate or prevent Alzheimer's Disease.
EP0944610B1 Asymmetric synthesis of benzoxazinones The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
US20130023486 Phenyl c-glucoside derivatives, preparation methods and uses thereof The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof, wherein, the definitions of R5 and R6 are selected from the following: (1) R5=R6=Me; (2) R5=Me, R6=OMe; (3) R5=Me, R6=H; (4) R5=Me, R6=F; (5) R5=F, R6=H; and (6) R5=OMe, R6=H.
WO2006089803A1 Method and composition to inhibit infections with helicobacter pylori by intake of procyanidins from type b and c Methods and compositions, including, foods and beverages, for treating, preventing or ameliorating Helicobacter pylori-associated disorders, particularly disorders of the gastrointestinal tract such as peptic ulcers of the stomach are provided by this disclosure. In one preferred aspect, the method comprises administering to a Helicobacter pylori infected subject a therapeutically effective amount of a composition comprising Type-B procyanidins, Type-C procyanidins, or a mixture thereof.
CN102526023A Application of EGCG (epigallocatechin gallate) in preparing medicine for treating type-II diabetes The invention discloses application of EGCG (epigallocatechin gallate) in preparing a medicine for treating type-II diabetes, relates to the field of biology and medicine, and aims to provide an application of EGCG in treating the type-II diabetes. The major technical characteristics are as follows: EGCG can be used for effectively preventing and treating the type-II diabetes and the associated mitochondrial dysfunction in myocardial cell, autophagy increase and oxidative stress up-regulation; and EGCG prompts that the inhibition of EGCG on insulin resistance is possibly realized by inhibiting the regulation of F0x01 on autophagy, and prompts that F0x01 is possibly a target for treating diabetes.
US20090118312 flavivirus antivirals based on1,6-diazacyclotetradecane with fused pyrrolidine or cyclopentane ring at positions 3,4 and methylene bridge at positions 7,8; macrocyclic ring substituted with quinazolin-4-yloxy substituent on the fused pyrrolidine or cyclopentane ring Compounds of the formula I: and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(═O)pR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; — denotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl-carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV
US20080287390 Pyrazolidinol compounds The invention provides the use of an optionally hydroxyl-protected 4-hydroxy or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in drug therapy or prophylaxis. Additionally, the invention provides a method of combating HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient.
US20100267663 A composition for cicatrisation processes in the treatment of hypertrophic scars and for improving the biomechanical properties of the cutis This invention concerns a composition for pharmaceutical and/or cosmetic and/or in the form of medical device, in particular for the prevention and treatment of hypertrophic scars and/or cheloids, to inhibit any fibrosclerotic process and to improve the biomechanical properties of the skin and to obstruct retraction to cicatrisation of the skin, as it contains, as an active ingredient, at least one of the active principles chosen between fucose (and/or Fucose rich polysaccharides—FROPs), Dimethyl sulfone and acetyl glucosamine.
WO2013024487A1 Anti- vitiligo composition The invention deals with a novel composition for the treatment of vitiligo comprising of: : Benzyl peroxide, Precipitate Sulphur, Clobatesol dipropionate and Trioxaralen.. The ingredients and the concentrations of the ingredients of composition are selected in way to provide superior efficacy and safety even on prolonged use as well as to care of serious adverse effects like atrophy observed with the use of potent steroids.
US20100204175 Use of conjugates of hyaluronic acid in the local treatment of hyperproliferative skin diseases The use is described of a conjugate between hyaluronic acid or a derivative thereof and antitumoral drugs for the preparation of pharmaceutical compositions for the topical treatment of hyperproliferative skin diseases.
WO2009095445A1 New second medical use of 3-(2,2,2-trimethylhydrazine)propionate dihydrate The present invention relates to use of 3-(2,2,2-trimethylhydrazinium)propionate dihydrate for the treatment of impotentia generandi.
CN101336077A Use of 25-hydroxy vitamin D3 to improve vitality of animals The present invention relates to the use of 25-hydroxy-vitamin D3 to improve the general health status of female animals at least during gestation and/or lactation. The invention also relates to the use of 25-hydroxy-vitamin D3 in animal breeding. More particular, the invention relates to the use of 25-hydroxy-vitamin D3 for improving litter size and vitality of piglets in pig breeding and for providing better body frame and increasing gestation backfat gain, reducing lactation backfat loss and increasing lactation feed intake of sows and gilts.
CN103054870A Use of tryptanthrin compound as indoleamine 2,3-dioxygenase (IDO) inhibitor The invention belongs to the medicinal field, and concretely relates to a use of a 8-nitrotryptanthrin compound as an IDO inhibitor. The 8-nitrotryptanthrin compound is a reversible IDO inhibitor, has an inhibition constant Ki of 0.054muM, has in-vitro and cell-based median effective inhibition concentrations IC50 of 0.103muM and 1.80*10<-5>muM respectively, and has an inhibition effectiveness obviously better than a present inhibitor 1-methyltryptophan (Ki of 34muM and IC50 of 340muM). 8-nitrotryptanthrin disclosed in the invention can effectively lower the abnormally-increasing IDO activity in a tumor animal model as the IDO inhibitor, and also has tumor treatment effects comprising tumor growth delaying, tumor volume reduction and in-vitro tumor cell killing. 8-nitrotryptanthrin disclosed in the invention has a wide application prospect, and can be used for treating serious diseases having the IDO mediated tryptophan metabolism approach pathology characteristics, such as cancers, the Alzheimer disease, tristimania, cataract and the like as the IDO inhibitor.
US7378532 Anticancer agents; such as succinic acid mono-[5-(1-benzyl-1H-indazol-3-yl)-furan-2-ylmethyl]ester, sodium salt; inhibit cancer cell growth A fused pyrazolyl compound of the following formula: wherein A, Ar1, Ar2, R1, R2, R3, and R4, are as defined herein. Also disclosed is a pharmaceutical composition containing an effective amount of the above-described fused pyrazolyl compound.
EP0817621B2 Pharmaceutical composition for transdermic delivery A pharmaceutical composition for transdermal delivery including (a) optionally a polymeric release matrix capable of forming a flexible film when dried, said matrix being selected from cellulose polymers or copolymers and vinylpyrrolidone/vinyl acetate copolymers, (b) an active principle, (c) a transcutaneous absorption promoter for the active principle, and (d) a physiologically acceptable non-aqueous solvent capable of dissolving the release matrix, the active principle and the transcutaneous absorption promoter, and quickly removing same by evaporation on contact with the skin.
CN101057865A Method for preparing 'youkadan' granule The invention discloses a process for preparing pediatric paracetamol and amantadine hydrochloride granules for treating children's common cold, wherein each unit of the preparation comprises Paracetamol 100mg, amantadine hydrochloride 40mg, artificial ox gallstone 4mg, caffeine 6mg and chlorpheniramine maleate 0. 8mg.
WO2006069098A1 Nanoparticulate bicalutamide formulations The present invention is directed to compositions comprising an acylanilide, such as bicalutamide, having improved solubility in water. The bicalutamide particles of the composition have an effective average particle size of less than about 2000 nm, and are useful in the treatment of prostate cancer.
CN101472573B Reduced coenzyme Q10-containing composition and method for producing the same The present invention provides a particulate composition wherein an oil component containing reduced coenzyme Q10 is polydispersed forming a domain in a matrix containing a water-soluble excipient, which simultaneously shows high oxidative stability and high oral absorbability, a production method thereof, and a stabilizing method thereof. It also provides a food, food with nutrient function claims, food for specified health uses, dietary supplement, nutritional product, animal drug, drink, feed, pet food, cosmetic, pharmaceutical product, therapeutic drug, prophylactic drug and the like, which contain the composition.
CA1341482C Process for preparing fragments of aids-associated retroviruses Recombinant hTLR proteins are made using expression vectors containing DNA constructs derived from ARV-2 nucleic acid. These proteins ate useful in serological immunoassays to detect antibodies to hTLR.
CN102302491A Application of sorafenib to treatment of cerebral vasospasm (CVS) after subarachnoid hemorrhage (SAH) The invention discloses application of sorafenib shown in a formula (I) to the preparation of a medicinal composition for treating cerebral vasospasm (CVS) after subarachnoid hemorrhage (SAH). Animal experiments prove that BAY 43-9006 has the effect of obviously inhibiting the CVS after the SAH, and can be used for improving the CVS after the SAH.
US7919098 ErbB-3 based methods and compositions for treating neoplasms The present invention relates to compositions and methods for treating neoplasms in mammals, particularly humans. More particularly, the present invention provides for methods for preventing, treating or delaying neoplasm in a mammal using an ErbB-3 protein, a nucleic acid encoding an ErbB-3 protein or a functional fragment thereof. The present invention also provides for isolated nucleic acids encoding an extracellular domain of the ErbB-3 protein, or a functional fragment thereof, substantially purified extracellular domain of the ErbB-3 protein, or a functional fragment thereof and antibodies that bind to an epitope in an extracellular domain of the ErbB-3 protein, or a functional fragment thereof. The present invention further provides for pharmaceutical compositions and/or vaccines comprising the extracellular domain of the ErbB-3 protein, or a functional fragment thereof, or nucleic acids encoding and antibodies binding to such extracellular domain or functional fragments thereof.
EP2005951A9 Agent for improving nervous system cell functions The present invention aims to activate neural cells in brain, and further provide a useful composition having an action to protect intracerebral neural cells from external and internal stresses. An agent for improving a neural cell function containing reduced coenzyme Q as an active ingredient, more specifically, an agent for activating neural cells and an agent for protecting neural cells, is useful, and can be used for the improvement or prophylaxis of central neurological diseases or neuropathy symptoms derived from or associated with a neurodegenerative disease, promotion of cognitive function or improvement of learning and memory disorders.
CA2175054C 2-(pyrazol-3-yl)carbapenem derivatives A compound of formula (I) in which R is (a), wherein R.alpha. is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; R.beta. is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; or R.alpha. and R.beta. together form an optionally substituted 5- or 6-membered heterocyclic ring with or without additional heteroatoms; R1 is (C1-6)alkyl which is unsubstituted or substituted by fluoro, a hydroxy group which is optionally protected by a readily removable hydroxy protecting group, or by an amino group which is optionally protected by a readily removable amino protecting group; R2 is hydrogen or methyl, and -CO2R3 is carboxy or a carboxylate anion or the group R3 is a readily removable carboxy protecting group. Compounds of formula (I) which include pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolysable esters thereof have a broad spectrum of anti-bacterial activity and show good stability towards DHP-1.
DE102010027595A1 Clinical application of adenosine derivative, preferably (dihydroxyphenyl)ethyl-amino-purin-9-yl-(hydroxymethyl)oxolane-diol, for reducing body temperature during impending ischemia of brain vessels, which occur during heart attacks Clinical application of adenosine derivative (II), preferably (5R)-2-(6-{[2-(3,4-dihydroxyphenyl)ethyl]amino}-9H-purin-9-yl)-5-(hyd roxymethyl)oxolane-3,4-diol, for reducing body temperature during impending ischemia of brain vessels, which occur during heart attacks and strokes after accidents, preferably drowning accidents and during prolonged surgical interventions, preferably cardiac operations, is claimed. Clinical application of adenosine derivative of formula (II), preferably (5R)-2-(6-{[2-(3,4-dihydroxyphenyl)ethyl]amino}-9H-purin-9 -yl)-5-(hydroxymethyl)oxolane-3,4-diol, for reducing body temperature during impending ischemia of brain vessels, which occur during heart attacks and strokes after accidents, preferably drowning accidents and during prolonged surgical interventions, preferably cardiac operations, is claimed. R1 : H, NH 2or OH; and R2 : CH 2OH, CH 2OR 3, CH 2PO(OH) 2, CH 2OPO(OH)OX, CH 2POO(OH)O ->HNR 3 +>; X : Na, K, Li, N(R3)4 or lysine; R3 : Me, Et, (CH 2) 2OH or O(CH 2) 2O(CH 2) 2OH, and R4 : H, acetyl, OCOEt or COC 17H 35. [Image] - ACTIVITY : Antipyretic. No biological data given. - MECHANISM OF ACTION : None given.
CN101054382A Gamboges acid derivative, process for producing the same, and use thereof The present invention discloses a gambogicacid derivative and its preparation method. The derivatives comprises multiple amino acid residue and salt made from derivative and acid and alkaline. Biological test testifies that the gambogicacid derivative possess anticancer activity and can be used as anticancer drug or as precursor compound for seeking for anticancer drug.
CN1876168A Soup formulation medicine for treating recurrent ulcerative stomatitis and preparation method thereof Disclosed is a medicinal broth for treating ulcerative stomatitis and its preparing process, wherein the medicament is prepared from the following raw materials (by weight portion): ledebouriella root, cape jasmine, wrinkled giant-hyssop, fresh ginger, lilyturf root, capsule of weeping forsythia each 8-10g, calcium sulphate 15-18g, atractylodes rhizome, lotus leaves each 4-5g.
WO2012034954A1 Substituted hexahydropyrrolo [1, 2 - c] imidazolones useful as mdm2 inhibitors There are provided compounds of formula I (I) or a pharmaceutically acceptable salt thereof, wherein X, Y, R1, R1', R2, R2', R3, R4, R5 are as defined herein, methods of making those compounds as well as their use as medicaments, in particular as medicaments in the treatment of cancer.
WO2013172872A1 Pyrimidine diamine derivatives as inhibitors of cytosolic hsp90 The present application describes organic compounds that inhibit the activity of cytosolic heat shock protein Hsp90. Also described are methods useful for prophylaxis, treatment, or amelioration of symptoms of diseases or conditions that are responsive to inhibition of Hsp90 activity, such as neurological diseases, proliferative disorders, and infection.
CA2565431C Antibiotic compound produced by fermentation with streptomyces sp. Fermentation of a nutrient medium with a eubacterium Streptomyces sp. yields a novel antibacterial compound of structural formula (I).
WO2012119077A1 Co -administration of eribulin and farletuzumab for the treatment of breast cancer The present invention provides methods for treating a subject having breast cancer by administering (a) eribulin or a pharmaceutically acceptable salt thereof, and (b) farletuzumab or an antigen-binding fragment thereof.
US20120115808 Pharmacological preparation for topical use containing n-palmitoyl-vanillamide The present invention relates to topical preparations containing N-palmitoyl-vanillamide having hyperalgesic activity. In particular, the invention relates to N-palmitoyl-vanillamide for use in the treatment of pathologies selected from: post-herpetic neuralgia, neuralgia of trigeminus, occipital neuralgia, dental neuralgia, glottopharyngeal neuralgia, uremic neuralgia, diabetic neuralgia, headache of different origin, neuropathic itch, neurogenic itch, uremic itch, vulvodinia, vulvar vestibulitis, ano-rectal pain and itch, balano-preputial pain and itch, painful urogenital disorders of dogs and cats, psoriasis-associated pruritus and pain, itching skin diseases (e.g. atopic dermatitis) in the human and veterinary field, muscular pain, pain of the tendon, osteoarthritis associated pain in humans, dogs and cats; painful eye diseases in the human and veterinary field, inflammatory pathologies of the oral cavity in the human and veterinary field.
WO2013066903A1 Combinational liposome compositions for cancer therapy The present invention provides methods for delivery of therapeutic agents to a subject using multi-component liposomal systems. The methods include administration of a therapeutic liposome containing an active agent, followed by a administration of an attacking liposome that induces release of the agents from the therapeutic liposome.
WO2012010977A8 Single daily dosage form for prevention and treatment of metabolic syndrome The present invention is in the fields of medicine, pharmaceuticals, nutraceuticals, endocrinology and cardiology. The invention provides compositions comprising a statin, an inhibitor of the angiotensin converting enzyme, an antiplatelet compound and an anti- hyperglycemic compound for use in the treatment and/or prevention of cardiometabolic risk factors of Metabolic Syndrome and treatment and/or prevention of Metabolic Syndrome. The present invention provides for the use of such compositions in the manufacture of products for treatment and/or prevention of Metabolic Syndrome. The biguanide metformin of the composition could be present in extended release form allowing its use together with the other drugs in a single dosage form at low dose. This combination of drugs in a single daily dosage greatly improves compliance and adherence to treatment which is a critical factor for treating patients with Metabolic Syndrome.
US7501135 Gastric acid secretion A method of reducing gastric acid secretion in animals including humans comprising administering an extract of a plant of the genus Hoodia or Trichocaulon to animals, generally mammals.
CN102066365A Thiophene or thiazole derivatives and their use as PI3K inhibitors This invention provides compounds of formula (I) wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
CN101524353A Oral anti-allergy compound pharmaceutical composition The invention relates to an oral anti-allergy compound pharmaceutical composition, which contains levocetirizine and mast cell membrane stabilizer. The dosage forms of the composition comprise tablet, capsule, suspending agent, dry suspending agent, oral solution, granule, and the like. The oral medicament is applied to the treatment of allergic diseases such as urticaria, eczema, dermatitis, allergic rhinitis, skin pruritus, and the like.
CA2375008C Phenoxypropylamine compounds The present invention relates to a phenoxypropylamine compound of the formula (I) (see formula I) wherein each symbol is as defined in the specification, an optically active compound thereof or a pharmaceutically acceptable salt thereof and hydrates thereof, which simultaneously show selective affinity for and antagonistic activity against 5-HT1A receptor, as well as 5-HT reuptake inhibitory activity, and can be used as antidepressants quick in expressing an anti-depressive effect.
US6872751 Composition and method for augmenting or restoring the production of fetal protein in patient in need thereof The present invention relates to methods for prevention and/or treatment of diseases or conditions caused by deficiency in the adult isoform of a given protein wherein said method comprises administering to a patient in need thereof a composition containing NO or at least one compound able to release, induce and/or promote NO formation in cells, said administration resulting in augmenting or restoring the production of the fetal isoform of said protein in said patient.
US20130079338 Selective NR2B Antagonists The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
WO2011044746A1 Bamboo or wood vinegar solution, preparation method and use thereof A bamboo or wood vinegar solution, preparation method and use thereof, said bamboo or wood vinegar solution comprises edible water 89-99%, organic acids 0.5-10%, flavonoids derived from bamboo leaves 0.05-0.20%, alcohols 0.05-1.6%, and water soluble flavors 0.05-0.20%. Impurities and toxic irritant substances and carcinogenic substances are removed from the bamboo or wood vinegar solution. The bamboo or wood vinegar solution has aroma.
US7820169 inhibiting the activity of tumor necrosis factor TNF in a patient having rheumatoid arthritis or psoriatic arthritis, by administering a composition comprising an effective amount of human anti-TNF antibody comprising a heavy chain variable region comprising SEQ ID NO:7 and a light chain variable The present invention relates to inhibiting TNF in patients having rheumatoid arthritis, psoriatic arthritis or ankylosing spondilitis, by administering anti-TNF antibodies comprising the heavy chain variable region of SEQ ID NO: 7 and the light chain variable region of SEQ ID NO:8, specific for at least one human tumor necrosis factor alpha (TNF) protein or fragment thereof.
WO2010071852A3 Oligonucleotide micelles The present invention provides homogenous populations of micelles, methods for preparing these populations, methods for treating or preventing a disease or disorder using the population of micelles of the invention.
CN1864725A Method for extracting active ingredient of starofbethlehem and use thereof The invention provides a process for preparing Ornithogalum caudatum Ait saponin through mega-aperture resin extraction, and the use in the preparation of medicaments for treating hepatic carcinoma, lung carcinoma, gastric carcinoma and mammary cancer.
US20100222350 Phenyl, pyridine, quinoline, isoquinoline, naphthyridine and pyrazine derivatives This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
CN103027930A Biomass composition capable of forming and slowly releasing short-molecular polysaccharide, preparation method and preparation thereof The invention discloses a biomass composition capable of forming and slowly releasing short-molecular polysaccharide, a preparation method and a preparation of the biomass composition. The biomass composition capable of forming and slowly releasing short-molecular polysaccharide comprises the following components in part by weight: 50-300 parts of Poria cocos and 20-80 parts of acidic material. The preparation method of the biomass composition comprises steps of pretreatment, blending, sterilization and split charging, in particular comprises the following steps: removing impurities from Poria cocos, rinsing and cutting Poria cocos, and performing superfine grinding to Poria cocos for future use; adding the superfine ground acidic material into the treated Poria cocos, mixing the acidic material and Poria cocos uniformly to obtain the target composition; and sterilizing the target composition and carrying out split charging. The preparation of the biomass composition is a powder, a capsule, a granule, a tablet or a pill prepared by adding a pharmaceutically acceptable auxiliary material into the slow-release drug with short-molecular polysaccharide. The biomass composition is simple in manufacturing process, convenient to operate, low in cost, convenient to take, high in absorptivity and long in timeliness.
WO2009085270A3 Use of inhibitors of c0nnexin43 for treatment of fibrotic conditions Treatment of fibrosis and fibrotic diseases, disorders, and conditions, and associated methods, compositions, formulations and articles.
WO2008095847A1 Bicyclic heterocycles, drugs containing said compounds, use thereof, and method for production thereof The invention relates to bicyclic heterocycles of general formula (I), wherein Ra, Rb and Rc are defined as in claim 1, to the tautomers thereof, the stereoisomers thereof, the mixtures thereof and the salts thereof, especially the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, especially an inhibitory effect on tyrosinkinase-mediated signal transduction. The invention also relates to the use of said compounds in the treatment of diseases, especially of tumors and of benign prostatic hyperplasia (BPH), lung diseases and respiratory tract diseases, and to the production thereof.
US7223837 Anticancer prodrugs, enhance enzymatic activation rates This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V—(W)k—(X)l—A—Z, wherein: V is a specifier; (W)k—(X)l—A is an elongated self-elimination spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclization elimination spacer; Z is a therapeutic drug; k, l and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: —when A is (Y)m: k+l+m≧1, and if k+l+m=1; —when A is U: k+l≧1.
CN101224211A Entecavir solid dispersoid, medicine compounds and preparing method and applications thereof The invention relates to a solid dispersion containing entecavir and any one or more components of polyethylene glycol, glycerin monostearate, polyoxyl stearate, sucrose ester of fatty acid and polyoxyethylenated castor oil and well overcomes the shortages of poor water solubility and dissolution of entecavir and is beneficial for the preparation of the medicine preparation and improving medicine quality. The invention also relates to the preparation, the medicine combination and the medicine application of the solid dispersion containing the entecavir and the carrier materials.
US20110271356 Hcv entry factor, occludin The human Occludin protein is identified as an essential Hepatitis C Virus (HCV) cell entry factor. Occludin is shown to render murine and other non-human cells infectable with HCV and to be required for HCV—susceptibility of human cells. Associated methods for inhibiting HCV infection, transgenic animal models for HCV pathogenesis, methods of identifying compounds or agents that prevent or mitigate interaction of HCV with Occludin, and HCV inhibitory agents are also disclosed. Kits and cell culture compositions useful for identifying compounds or agents that prevent or mitigate interaction of HCV with Occludin are also provided.
CN103373988A 1, 2, 4-Triazole and pyrazine ring-containing acylhydrazone derivatives, preparation method and applications Provided are 1, 2, 4-triazole and pyrazine ring-containing acylhydrazone derivatives which are characterized by the following general formula:, wherein R is for. The 1, 2, 4-triazole and pyrazine ring-containing acylhydrazone derivatives have obvious inhibiting effects on human lung cancer cells A549, human liver cancer cells HepG2, human breast cancer cells MCF7 and human stomach cancer cells SGC7901, so the 1, 2, 4-triazole and pyrazine ring-containing acylhydrazone derivatives can be applied to preparation of anti-cancer drugs. The invention discloses a preparation method for the derivatives.
EP1090011A4 Inhibitors of prenyl-protein transferase The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
US7700569 Single- or double-stranded stabilized DNA contains nonmethylated octameric CG motif of the sequence AACGTTAT (nucleotides 9-16 of SEQ ID NO: 9); phosphorothioate oligonucleotides; nuclease inhibitors; immunostimulants; nontoxic; anticarcinogenic agents; intratumoral administration; nervous systems The invention concerns the use of stabilized oligonucleotides comprising at least an octamer motif of the type: 5′-purine-purine-CG-pyrimdine-pyrimidine-X1X2-3′ wherein the pair X1-X2 is AT, AA, CT or TT, for preparing a medicine with antitumour activity.
CN101032564A Health preserving wine for conditioning blood-fat and the preparing method The present invention discloses one kind of blood fat regulating health wine, which includes white liquor and puerarin, resveratrol, resveratrol glycoside and/or ursolic acid. Each 500 ml of the health wine contains at least 1 mg of the said health factors. The blood fat regulating health wine is mellow, stable and controllable in quality, and has the health function of preventing and treating atherosclerosis.
WO2013055771A1 Thioxothiazolidinone derivatives useful as inhibitors of tdp1 Tdp1 inhibitors of Formula (I) and methods of using those inhibitors to treat cancer are provided in this disclosure. R1 is hydrogen or lower alkyl and G is a substituted phenyl or optionally substituted heteroaryl group. The disclosed Tdp1 inhibitors may be used alone to treat cancer, but may also be used in combination with another active agent, such as camptothecin or a camptothecin analogue.
EP2736898A1 5ht1a antagonist useful for in vivo imaging The present invention provides a novel compound of formula (I) useful for in vivo imaging of 5-HT1 A receptors in a subject. Also provided by the present invention is a precursor compound useful in the preparation of the compound of the invention, as well as said method of preparation. The present invention additionally provides methods for the use of the compound of the invention in an in vivo imaging method, and use of that in vivo imaging method in diagnosis and therapy monitoring.
CN101361724A Trimebutine or its salt sustained release capsules and preparation method thereof The invention discloses a slow release capsule of trimebutine or the salt thereof and a preparation method thereof. The slow release capsule of trimebutine or the salt thereof is prepared by adding the accessories of filler, adhesive and slow release materials and the like into the trimebutine, wherein, the trimebutine can be replaced by the maleate thereof or other medicinal salts. The slow release capsule of trimebutine or the salt thereof can be obtained through the following preparation processes: a pill core is first prepared by adopting microcrystalline cellulose or starch and the like through centrifugation, spray cementing, powder supply, polishing and other processes and coated with a medicated layer to prepare a medicated pill core, which is then coated with a slow release film to make a trimebutine slow release mini-pill, finally the slow release capsule of trimebutine or the salt thereof is obtained after filling the mini-pill in a capsule. Compared with the common preparation, the slow release capsule can continue with drug delivery for up to 12 hours, and has comparably stable blood concentration and long time to peak. And the preparation method of the capsule is characterized by good repeatability and easy operation and the like.
CN102600165A Application of compound alfuzosin hydrochloride in preparing information therapy medicines, preparation method thereof and prepared novel medicine The invention discloses application of compound alfuzosin hydrochloride in preparing information therapy medicines, a preparation method thereof and a prepared novel medicine. The information therapy medicines are not directly contacted with the human body when being used for therapy, medicine substance components are not consumed, only medicine information is utilized for physical therapy, the effect of chemical therapy can be achieved, a therapy window is expanded by more than one thousand times, and the side effects of the chemical therapy are avoided. After the alfuzosin hydrochloride is used as the information therapy medicine, and the contents of effective components of the alfuzosin hydrochloride are not changed. The alfuzosin hydrochloride also can be used as a conventional chemical therapy preparation to be reused effectively.
WO2012006760A1 Tricyclic compounds as allosteric modulators of metabotropic glutamate receptors The present invention describes and claims compounds of the Structural Formula (I), Structural Formula (II), or Structural Formula (III). In Formula (I), R1, R2, R3 and R3' are -H or methyl, or R3 and R3' taken together form a double bond, or R3' is -H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is -H or -F, and R5 is -H, methyl, -Cl or -Br. In Formula (II), R1 is -H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is -H or -F, and "Y" is: (a) -CH2-; (b) -CR6H-O-CR7R8-, wherein R6, R7, and R8 are independently -H or methyl; (c) -CR6H-N(R9)-CR7R8-, wherein R6, R7, and R8 are independently -H or methyl; (d) -CH2-C(R9)(R10)-C(R7)(R8)-, wherein R7, R8, R9 and R10 are independently -H or -methyl, or both R7 and R8 are -F, R9 and R10 are independently -H or -methyl, or both R9 and R10 are -F, or R9 and R10 taken together are (O=), which together with the carbon to which they are attached forms a carbonyl group.
EP2398806A1 (+)-morphinanium n-oxides and processes for their production The present invention provides (+)-morphinanium N-oxide compounds or pharmaceutically acceptable salts thereof. The invention also provides processes for producing (+)-morphinanium N-oxides or pharmaceutically acceptable salts thereof from the corresponding tertiary N-substituted (+)-morphinan compound or pharmaceutically acceptable salt thereof.
US20100144718 Treatment of diseases modulated by a h4 receptor agonist The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.
US7521443 3,8-Diazabicyclo[3.2.1]octane-3-carboxylic acid, 8-[[8-cyclohexyl-5-[[[(dimethylamino)sulfonyl]amino]carbonyl]-1,12b-dihydro-11-methoxycycloprop[d]indolo[2,1-a][2]benzazepin-1a(2H)-yl]carbonyl]-, phenylmethyl ester; RNA polymerase inhibitor; liver disease, including cirrhosis and hepatocellular carcinoma The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
CN1568948A Venlafaxine hydrochloride drop pills and preparation method thereof The invention discloses am venlafaxine hydrochloride drop pill prepared through ultramicro disintegration and drop pills manufacturing technique, which has the advantages of improving collapse and dissolving speed, dissolving out speed and degree, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use. It has good compliance, thus is especially suitable for children, the elderly, bedridden patients and dysphagia patients.
WO2009066072A3 Inhibitors of 17beta-hydroxysteroid dehydrogenase There is provided a compound having Formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, -OC(R13)3, -OCH(R13)2, -OCH2R13, -C(R13)3, -CH(R13)2, or -CH2R13 wherein R13 is a halogen; (c) -CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (I) aryloxy; (m) -SO2-alkyl; and (n) -N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (T) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=O, S(=O)2, C=O, S(=O)2NR16, C=ONR17, NR18, in which R16, R17, and R18 are independently selected from H and hydrocarbyl, R10 is selected from H and hydrocarbyl, R11 is selected from CR19R20 and C=O, in which R19 and R20 are independently selected from H and hydrocarbyl, R12 is selected from a substituted five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring, and wherein the one or more substituents are selected from hydrocarbyl groups.
WO2005033102A2 Thiophene-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof Thiophene-based compounds of formula (I) exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed. These compounds are useful in the treatment of Alzheimer’s disease, stroke, diabetes, obesity, inflammation and cancer.
US20100239657 Composite for liver-specific delivery and release of therapeutic nucleic acids or drugs The inventive composite having a nanoscale particle size can specifically deliver therapeutic nucleic acids or drugs to the liver and selectively release them into hepatic cells to manifest potent therapeutic effects without inducing any enzymatic abnormalities or pathological damage to the normal liver function, when administered together with the therapeutic agents.
CN101700308A Paste for treating hyperosteogeny The invention relates to a paste for treating hyperosteogeny, which is characterized by comprising the following compositions in parts by weight: 10 to 20 parts of colophony, 0.1 to 1 part of gelatin, 0.1 to 1 part of scallion, 10 to 30 parts of far infrared ceramic powder, 0.5 to 2 parts of chili oil, 1 to 2.5 parts of pepper, and 1 to 2 parts of xylogen powder. The paste has the advantages that the prescription adopts pure natural substances extracted from plants and animals as raw materials, and uses the unique decocting and coating technology. The paste can be used conveniently and quickly without being baked; novel composite base materials are used to play drug efficacy continuously and uniformly; the paste has no stimulation to human body, does not contain red lead, has little toxic and side effects and no obvious allergic reaction, and the stimulation index is only 1.75 by using the method of identifying and testing average sensibilin; the paste can be pasted repeatedly; the paste gives off delicate fragrance, plays roles of activating blood, dissolving stasis, promoting microcirculation for cervical vertebra, lumbar, legs, joints, calcaneus and other parts of the human body and plays an assistant effect by combining with the corresponding physical therapy.
CN101392013A Ginsenoside Rb1 containing impurity ginsenoside Rh1 The invention discloses a standard ginsenoside Rb1 active ingredient, which contains ginsenoside Rb1 with the content more than or equal to 90 percent and smaller than 100 percent, and is characterized in that the content of impurity ginsenoside Rh1 is more than 0 and smaller than 5 percent; or the content of the impurity ginsenoside Rh1 is more than or equal to 0.1 percent and smaller than 5 percent; or the content of the impurity ginsenoside Rh1 is more than or equal to 0.5 percent and smaller than 3.0 percent; the pharmacological test shows that the active ingredient of the application has good pharmacological action, and can be prepared to pharmaceutical preparation in pharmacy.
US8106185 Agmatine or aminoguanidine and dextran hydroxypolymer, Tc-99m radionuclide, Farmorubicine anticancer drug, Tamoxifen; intravesically, regiolocally, peritoneally, intratumorally, systemically or intravenously administrable The present invention is related to a modified hydroxypolymer conjugates preferably a guanidine-dextran conjugate having a tumor cell killing activity. The modified hydroxypolymer conjugate is used as medicine, particularly for manufacturing a medicine or tumor killing composition for treating tumors. A method for producing said hydroxypolymer conjugate and a method for killing cancer cells and treating tumors is also disclosed. The invention is also related to a method for killing tumor cells and treating tumors by administering an effective amount of the modified hydroxypolymer conjugate.
US20130085176 Process for the preparation of sulfamide derivatives The present invention is directed to a process for the preparation of sulfamide derivatives.
CN101698039A Ganji san and preparation method thereof The invention discloses Ganji san and a preparation method thereof; the ingredients of the Ganji san are as follows by weight parts: 3-10 parts of rangooncreeper fruit, 3-10 parts of Chinese gall, 3-10 parts of sea squirt, 3-10 parts of liquorice, 3-10 parts of narcissus, 3-10 parts of semen brassicae, 3-10 parts of common yam rhizome, 3-10 parts of red orpiment, 0.1-1 part of cinnabar and 0.1-0.6 part of mercurous chloride; the preparation steps of the Ganji san are as follows: the rangooncreeper fruit, the Chinese gall, the sea squirt and the liquorice are placed in an oven for being baked for 1-3 minutes; and then the narcissus, the narcissus and the common yam rhizome are added in for being baked for 20-60 seconds and are taken out; the red orpiment is powdered, and is mixed with the cinnabar and the mercurous chloride and the other raw materials, and then the mixture is crushed; the powder is sterilized and is packed into bags with 5g each one.
US20130072540 RNA interference of galectin-3 expression and methods of use thereof Galectin-3 is a pro-inflammatory molecule functioning as a cytokine hub, and also regulates unfolded protein responses (UPR) and ER stress. Thus, galectin-3 serves as a target for ameliorating inflammatory diseases such as allergic inflammation and diabetic inflammation and insulin resistance. RNA interference of endogenous galectin-3 expression, upregulates IL-12, IL-10 while downregulating IL-23 production, which offers protection against allergic inflammation. In addition, endogenous galectin-3 knockdown causes upregulation of XBP1, alleviating ER stress. Together, upregulated XBP1 and IL-10 offer protection against obesity-induced inflammation. Therefore, the embodiment of the invention resides in RNA interference of endogenous galectin-3 in appropriate cell types in order to rectify allergic and/or diabetic inflammation.
US20120040916 Molecular inhibitors of the wnt/beta-catenin pathway The present invention is directed toward a method of treating a subject for a condition mediated by the Wnt/β-catenin pathway by selecting a subject with a condition mediated by the Wnt/β-catenin pathway and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly inhibiting the Wnt/β-catenin pathway in a subject is also disclosed.
CN103623423A Agomelatine inclusion compound and preparation method and application thereof The invention relates to an agomelatine inclusion compound and a preparation method and application thereof. The agomelatine inclusion compound comprises agomelatine and cyclodextrin or derivatives of cyclodextrin. The agomelatine inclusion compound is characterized in that the agomelatine inclusion compound does not have a melting point endothermic peak of agomelatine. According to the preparation method, the agomelatine is included or embedded into the cyclodextrin or derivatives of cyclodextrin through inclusion, thus forming the agomelatine inclusion compound. The agomelatine inclusion compound is in a novel agomelatine solid form, and the polymorphism or mixed crystal problem of the agomelatine can be effectively solved, so that the production process is simplified. Meanwhile, the inclusion compound has the advantages of high water solubility and high stability, and the preparation method is easy and convenient to operate, low in material consumption and low in cost. The invention also discloses application of the agomelatine inclusion compound in preparation of pharmaceutical preparations for treating depression. Therefore, the agomelatine inclusion compound has extremely practical value in development and application of agomelatine.
US20080249102 Hiv Protease Inhibitors Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A′ and A″ are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.
WO2010130779A2 COMBINATION OF A PBOSPBOINOSITKLE 3-KSπASE INHIBITOR AND AN ANTIDIABETIC COMPOUND The invention relates to a pharmaceutical combination which comprises (a) a phosphosnositide 3-kinase inhibitor compound and (b) an insulin sensitivity enhancer compound for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
WO2005094858A1 Antidiabetic composition It is intended to provide an antidiabetic composition containing an active ingredient originating in a natural plant which can be obtained and taken in daily diet, inhibits hyperglycemia after eating to thereby efficaciously relieve the onset of diabetes or the symptoms thereof, and is highly safe and less expensive. This object can be achieved by providing a preventive/remedy for diabetes and health foods containing, as the active ingredient, safflower (Carthamus tinctorius L.: an asteraceae) petal and/or an extract thereof or yellow colorants (safflower yellow) and red colorants (carthamine and safflomin A) contained in safflower petal.
US20090041859 Wound Treatment Drugs for External Use [Problems] The objective is to provide a new low-toxic drug for external use for intractable diseases, such as erosion, decubitus, and skin ulcer, that prevents cicatrization and reduces iodine accumulation on wound surfaces with sufficiently promoting healing. [Means for solving problem] Preparation of a wound treatment drug for external use containing oily bases and iodine but substantially no white soft sugar, which is a characteristic of the drug of this invention. The invented drug prevents infection through the wound surface due to a sufficient bactericidal effect of iodine, and promotes wound healing, prevents cicatrization and reduces iodine accumulation on the wound surface by maintenance of appropriate moisture in the wound surface due to a moisturizing effect of oily bases.
CN103550694A Medicine for treating alopecia and preparation method thereof The invention discloses a medicine for treating alopecia and a preparation method thereof. The medicine is mainly prepared from the following medicines in a certain percentage by weight: alum, radix curcumae, ruddle, hemp flowers, cockscomb, polygonum multiflorum, astragalus, codonopsis pilosula and semen sesami nigrum. The medicine has the effects of regulating qi-flowing for strengthening spleen, invigorating the kidney and strengthening Yang and clearing away heat and toxic materials, is fast in effectiveness and short in course of treatment when used for treating the alopecia, and the alopecia does not reoccur.
EP2191842A1 Antitumor combinations containing antibodies recognizing specifically CD38 and cytarabine Pharmaceutical composition comprising an antibody specifically recognizing CD38 and cytarabine.
WO2009089042A1 Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith Provided herein are Pyrazole Pyrazine Amine Compounds having the following structure:Formula (I). Wherein Q and R1-R3 are as defined herein, compositions comprising an effective amount of a Pyrazole Pyrazine Amine Compound and methods for treating or preventing inflammatory conditions, immunological conditions, cancer, neurodegenerative diseases, age-related diseases, cardiovascular diseases and metabolic conditions, or conditions treatable or preventable by inhibition of an IKK, or an IKK pathway, comprising administering an effective amount of a Pyrazole Pyrazine Amine Compound to a patient in need thereof.
CN103720686A Application of Trigoxyphin K in medicine for increasing red blood cells The invention relates to a novel application of a compound Trigoxyphin K in the field of pharmacy, and relates to an application of Trigoxyphin K in preparation of a medicine for increasing red blood cells. The application of the related Trigoxyphin K in the preparation of the medicine for increasing the red blood cells is disclosed for the first time. Due to the fact that a skeleton type belongs to a brand-new skeleton type, and further, inhibitory activity for low red blood cells is strong, outstanding substantive features are provided, and simultaneously, Trigoxyphin K makes remarkable progress for preventing and curing low red blood cells.
EP1879562A2 Phenol derivatives and their use to modulate pkb activity The present invention provides the use of a compound of the Formula: (I) wherein R1 is C1-5 alkoxy, OCOC1-3Alkyl, O(CH2)2O(CH2)2O(CH2)2OMe, O(CH2)2O(CH2)2O(CH2)2OH or OH; R2 is H, (CH2)nOH, OCH3, Hal or (II) or (III) R3 is H or (CH2)nOH; and R4 is C1-6 alkyl, optionally substituted by one or more of Hal, OH, COCH3, NH2, NHCH3, NHMe, NMe2, OCOCH3, CO2H or esters or amides thereof where n is 1-5; and pharmaceutically acceptable salts thereof, in the manufacture of a medicament for use in modulating PKB activity.
CN1820752A Oral liquor slow releasing preparation containing codeine and chlorophenamine and its preparing method The present invention discloses oral slow released liquid preparation containing codeine and chlorophenamine and its preparation process. The preparation has improved effectiveness, safety and compatibility, and suitable for children and old people to take. The preparation includes codeine, chlorophenamine, ion exchange resin, hydrophilic or water soluble material, coating material, plasticizer, suspension assistant and pure water. The preparation process includes the following steps: preparation of resin containing medicine, coating of resin containing medicine, and preparing suspension of resin containing medicine. Compared with available technology, the present invention has obvious slow release effect, reduced medicine taking times, less side effect, convenient taking and good taste, and is used in treating dry cough, and acute and frequent cough.
WO2013138236A1 2'- substituted carba-nucleoside analogs for antiviral treatment Provided are compounds of Formula I, as well as pharmaceutical compositions containing compounds of Formula I and methods for treating Orthomyxoviridae virus infections by administering these compounds. The compounds, compositions, and methods provided are particularly useful for the treatment of Human Influenza virus infections.
CN102406729A Normal temperature preparation method of ultrafine Maxingshigan powder and special bidirectional air flow screening machine for same The invention discloses a normal temperature preparation method of ultrafine Maxingshigan powder, which comprises the following steps of: firstly, selecting ephedra, bitter apricot seed, gypsum and liquorice root according to a certain proportion; after drying, grinding the raw materials and extracting bitter apricot seed oil from bitter apricot seed coarse powder for later use; after grinding the coarse powder in a rod mill, feeding the ground coarse powder into a special bidirectional air flow screening machine by the wind and sieving the ground coarse powder by using a 500-mesh sieve; conveying powder with the particle size of less than or equal to 25 microns, which is obtained by sieving, into a cyclone loading head by air flow generated by a draught fan to collect the powder so as toobtain the ultrafine Maxingshigan powder; collecting powder which is not sieved by using the 500-mesh sieve and conveying the powder into the rod mill to circularly grind the powder again; and sufficiently stirring the ultrafine Maxingshigan powder and the bitter apricot seed oil to obtain the finished product of the ultrafine Maxingshigan powder. The normal temperature preparation method has theadvantages that the integral preparation process is carried out at normal temperature; the prepared finished product medicament has particle size of less than or equal to 25 microns; and the cell-wall breaking ratio and the bioavailability are greatly improved. Due to the adoption of the bidirectional air flow screening machine in the normal temperature preparation method, the preparation processof the ultrafine Maxingshigan powder is simplified.
CN103070847A Method for preparing docusate sodium soft capsules The invention discloses a method for preparing docusate sodium soft capsules, which comprises the following steps: A, preparing red gelatin solution, i.e. dissolving a plasticizer into water, adding the obtained product into a gelatin melting tank, heating to a temperature of 40 to 80 DEG C, adding gelatin, stirring to dissolve the gelatin to obtain gelatin solution, adding a colorant I into the water, uniformly stirring, adding the mixture into the gelatin solution, stirring, vacuumizing and discharging air bubbles to obtain the red gelatin solution for later use; B, preparing white gelatin solution, i.e. adding an additive into the sufficient quantity of water, uniformly dispersing by a colloid mill to obtain solution I, dissolving the plasticizer into the water, adding the solution I and the plasticizer solution into the gelatin melting tank to heat to a temperature of 40 to 80 DEG C, adding gelatin, stirring and dissolving the gelatin, and after totally dissolving the gelatin, vacuumizing and discharging air bubbles to obtain the white gelatin solution for later use; C, preparing contents, i.e. adding polyhydric alcohol into polyethylene glycol solution of docusate sodium and uniformly mixing at a temperature of 30 to 50 DEG C to obtain the contents for later use; and D, preparing the soft capsules, i.e. adding the content liquor obtained in the step C into a feed hopper of a pelleting press, regulating packing volumes and thickness of shells, pelleting, drying, smearing pills and packaging.
US20090012120 Synthesis of N-heterocycles, beta-amino acids, and allyl amines via aza-payne mediated reaction of ylides and hydroxy aziridines An ylide-based aza-Payne rearrangement of 2,3-aziridin-1-ols leads to an efficient process for the preparation of pyrrolidines. The aza-Payne rearrangement under the basic reaction conditions favors the formation of epoxy amines. Subsequent nucleophilic attack of the epoxide by the ylide yields a bis-anion, which upon a 5-exo-tet ring closure yields the desired pyrrolidine, thus completing the relay of the 3-membered the 5-membered nitrogen containing ring system. This process takes place with complete transfer of stereochemical fidelity, and can be applied to sterically hindered aziridinols.
CN101507728A Composite for preventing and treating body acidification of diabetic The invention discloses a monomer or a composition for preventing and treating organism acidification of diabetics, and a preparation method and application thereof. Calculated as 100 weight portions of composition, the composition contains 1 to 100 weight portions of fiber pentose and 0 to 99 weight portions of sugar absorption enhancer, wherein the sugar absorption enhancer is selected from one or more of the following substances: cellulose, vitamin B1, vitamin B5, vitamin B6, thyroxine, adrenalin, potassium ions, magnesium ions, and sodium ions.
WO2005018625A1 Use of colipase-lipase inhibitors in the preparation of a pharmaceutical composition in order to prevent obesity The present invention relates to novel colipase-lipase inhibitors of the general formulae to be used in the treatment or prophylaxis of obesity, as well as pharmaceutical compositions containing the same, and method for treating obesity using said compounds.
CN102895228A Amoxicillin and sulbactam sodium medicinal composition injection and preparation method thereof The invention discloses an amoxicillin and sulbactam sodium medicinal composition injection and a preparation method thereof. According to a formula, the medicinal composition injection comprises the following components in part by weight: 1 to 10 parts of amoxicillin, 0.5 to 5 parts of sulbactam sodium, 0.4 to 8 parts of lactose, 0.4 to 8 parts of sodium chloride, and a proper amount of sodium dihydrogen phosphate, wherein sodium dihydrogen phosphate is used for regulating the pH value of a solution to be 7.0. The preparation method for the medicinal composition injection comprises the following steps of: weighing a certain amount of amoxicillin, sulbactam sodium, lactose and sodium chloride, dissolving by using water for injection, regulating the pH value of a solution to be 7.0 by using sodium dihydrogen phosphate, fixing the volume till 5,000ml by using water for injection, filtering by using a filtering membrane, drying, performing sterile crushing, and filling to obtain the amoxicillin and sulbactam sodium medicinal composition injection. The amoxicillin and sulbactam sodium medicinal composition injection prepared by the method has the advantages of low impurity content, high solubility and stability, difficulty in color change and the like.
WO2006064304A1 Acid addition salts of muscarinic receptor antagonists Provided herein are acid addition salts of muscarinic receptor antagonists. Such acid addition salts are muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. Also provided herein are processes for the preparation of acid addition salts, pharmaceutical compositions thereof, and methods of treating diseases mediated through muscarinic receptors.
CN1582935A Powder injections of namelfene and their preparation A powder injection or freeze-dried powder injection of nalmefen is prepared from nalmefen, aseptic water for injection, and auxiliaries.
CN1895668A Composite mucosa immunoadjuvant for oral vaccine A compound adjuvant for the mucosa immunization of oral vaccine is proportionally composed of soybean flavone, sodium fluoride and lactobacillus. It can improve the immunological competence and decrease the dosage of Newcastle disease IV vaccine.
WO2006046674A1 Preventive and remedy for hepatitis c virus infection A medicinal composition for preventing or treating hepatitis C virus infection which contains an extract of a plant belonging to the genus Polygala as the active ingredient. It is preferable that this medicinal composition contains an extract of Onji (root of Polygala Tenuifolia Willdenow) extract or Senega (root of Polygala senega Linne) extract. It is still preferable that the extract comprises a saponin such as onjisaponin or polygala saponin.
US7605162 Indole-3-alkyl-N-piperazine ring substituted with quinoline ring or derivatives; high affinity for both the dopamine D2 receptor and the serotonin reuptake site; nervous system disorders, such as anxiety disorders, depression, Parkinson's disease, and schizophrenia The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.
CN103446522A Medicine for treating acid regurgitation and preparation method of medicine The invention discloses a medicine for treating acid regurgitation and a preparation method of medicine. The medicine is mainly prepared from fructus amomi, myristica, hawthorn, medicated leaven, fructus aurantii and areca-nut according to a certain weight ratio. The medicine disclosed by the invention has the functions of tonifying spleen and harmonizing stomach, helping digestion and regulating middle energizer, relaxing muscle and clearing heat, and is used for treating acid regurgitation with fast effect and high cure rate.
WO2011161964A1 Agent for improving insulin resistance with acat inhibitor as active component In the present invention, a chemical compound having an insulin-resistance improving effect or a blood-sugar reducing effect is found, and a drug for the prevention and treatment of diseases caused by high blood sugar, such as diabetes, is provided. The present invention relates to a prophylactic or therapeutic agent for diabetes, and insulin resistance in particular, having an ACAT inhibitor as an active component thereof.
WO2009137404A1 Urea compounds as gamma secretase modulators The present invention provides compounds Formula (I) that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
CN101560265A Method for preparing oil-tea camellia husk polysaccharide and purifying method The invention discloses a method for preparing oil-tea camellia husk polysaccharide, and the method comprises the following steps: 1) oil-tea camellia husk powder is extracted by water at least once, the extracting solution is centrifugated or filtered, and the obtained supernatant is vacuum-concentrated, thus obtaining the concentrated solution; and 2) alcohol is added into the concentrated solution, then precipitation treatment lasts for 12 to 48 hours, then centrifugation is executed, the obtained precipitation is washed sequentially by absolute alcohol, absolute ether and acetone, after vacuum drying, the oil-tea camellia husk polysaccharide powder can be obtained. The invention also discloses a method for purifying the oil-tea camellia husk polysaccharide. The oil-tea camellia husk polysaccharide obtained by the method has the functions of anti-oxidation and anti-tumor.
US20100242127 Methods to identify modulators of b-raf protein kinase and their use for the treatment of anxiety and depression The present invention relates to a method for identifying a compound capable of modulating an anxiety or depression disorder comprising the steps of: (a) contacting a composition comprising a B-Raf protein or a B-Raf gene in expressible form or a transcript thereof with a compound under conditions that allow for an interaction of the B-Raf protein or the B-Raf gene or a transcript thereof and the compound; and (b) measuring whether said interaction, if any, results in (i) a change of B-Raf kinase activity compared to B-Raf kinase activity in the absence of said compound; (ii) a modulation of the expression of the B-Raf gene compared to B-Raf gene expression in the absence of said compound; or (iii) the formation of a complex between the compound and the B-Raf protein, wherein such a change in activity, modulation of expression or the formation of a complex is indicative of the compound being a modulator of an anxiety or depression disorder. Further, the invention relates to a method for treating an anxiety or depression disorder in an individual comprising administering to the individual an effective amount of a compound inhibiting B-Raf kinase activity or gene expression and to a use of a compound that inhibits B-Raf kinase activity or gene expression in the manufacture of a pharmaceutical composition for treating an anxiety or depression disorder. Moreover, the invention relates to a method of diagnosing a B-Raf associated anxiety or depression disorder and to a genetically engineered mouse. Finally, the invention also relates to a method of identifying another gene contributing to the pathophysiology of an anxiety or depression disorder apart from B-Raf.
CN102626409A Pharmaceutical composition containing 18 amino acids The invention discloses a pharmaceutical composition containing 18 amino acids. The pharmaceutical composition containing 18 amino acids is characterized in that raw materials of 18 amino acids and auxiliary materials of an antioxidant and a pH conditioning agent are prepared into compound amino acid injections (18AA-IV) having different concentrations, wherein the compound amino acid injection is the pharmaceutical composition containing 18 amino acids and has a pH value of 3.5 to 5.5. The pharmaceutical composition containing 18 amino acids does not contain a sulfite antioxidant and thoroughly prevents the damage of sulfites on the human body. Products of the pharmaceutical composition containing 18 amino acids are safer in clinical use. An accelerated stability test proves that the pharmaceutical composition (18AA-IV) containing 18 amino acids has the stability the same as or superior to the stability of commercial sulfite-containing like products.
US7553975 2-(((2-amino-1-oxo-3-mercapto-propyl)-amino)-methyl)-5-phenyl-thiazole-4-carbonyl-methionine; useful for treating restenosis or tissue proliferative diseases A family of compounds capable of inhibiting the activity of farnesyl transferase.
CN101244137B Medicament for treating pulmonitis, and high fever, lower fever, and preparation method The invention discloses a medicine for treating pneumonia and high/low fever as well as the preparation method, mainly comprising a Qingkailing injection, a ceftriaxone sodium for injection and an aminocaproic acid injection which are formed according to weight proportion. The medicine has the advantages of rapid curative effect and high healing rate in treating pneumonia as well as high/low fever.
CN101428022A Pantoprazole-containing medicament composition for treating peptic ulcer The invention relates to pharmaceutical composition containing pantoprazole for treating peptic ulcer. The pharmaceutical composition is characterized in that the composition comprises the following components: at least a helicobacter pylori inhibitor and at least a gastric acid secretion inhibitor. The helicobacter pylori inhibitor is selected from penicillin, penbritin, amoxicillin, metronidazole, furazolidone, erythromycin, erythromycin and the analog thereof, gentamycin and tetracycline, and the gastric acid secretion inhibitor comprises histamine receptor antagon, H<+>/K<+>-ATP enzyme (proton pump) and/or antacid. The composition can be produced into granules, effervescent tablets, tablets, capsules, syrup, injection, suspension injection, suppositories or sustained/controlled-release preparation, oral medicines or non-oral medicines, and can achieve the purpose of preventing and treating gastric ulcer and doudenal ulcer by effectively inhibiting the growth of helicobacter pylori and gastric acid secretion.
CN103301204A Compound fructus forsythiae-radix bupleuri oil nanoemulsion and preparation method The invention discloses a compound fructus forsythiae-radix bupleuri oil nanoemulsion, wherein the grain sizes of the liquid drops of the nanoemulsion range from 10 to 100 nm; and the nanoemulsion is prepared from the raw materials in the following percentage by weight: 12.00-28.00% of a surfactant, 15.00-30.00% of a cosurfactant, 3.00-8.00% of oil, 0.10-5.00% of fructus forsythiae oil, 0.10-5.00% of radix bupleuri oil, 0.01-0.05% of vitamin C, 0.01-0.05% of vitamin B, and 20.00-68.4% of distilled water, wherein the total percentage of the components is 100%. According to the compound fructus forsythiae-radix bupleuri oil nanoemulsion, the medicine stability of a fructus forsythiae oil and radix bupleuri oil mixture during a processing process can be improved, the bioavailability can be improved, the medicine metabolism time in a body can be delayed, the dosage of auxiliary materials can be reduced, and the production cost can be decreased; the compound fructus forsythiae-radix bupleuri oil nanoemulsion has a wide market prospect in the field of medicines.
US6861414 Methods for enhancing graft survival by modulating heme oxygenase activity Methods are provided wherein the survival of an organ transplant is enhanced by introducing into cells of the transplant a nucleic acid molecule that modulates heme oxygenase-I activity therein. Nucleic acid molecules that modulate heme oxygenase-I activity and therefore find use in the described methods include, for example, molecules that encode a polypeptide that itself exhibits heme oxygenase-I activity or antisense oligonucleotides that act to inhibit heme oxygenase-I activity in a cell.
US20060251675 Mutant cholera holotoxin as an adjuvant and an antigen carrier protein The invention relates to a mutant cholera holotoxin having reduced toxicity, which functions both as an adjuvant and an antigen carrier. In a particular embodiment, the cholera holotoxin is genetically modified at least at amino acid residue 29 of the A subunit, wherein the genetic modification comprises an amino acid substitution of the wild-type glutamic acid at position 29, wherein the substitution is not an aspartic acid.
US20130034510 Melanin modification compositions and methods of use A method for the modification of melanin distribution, and the composition thereof to modify melanin distribution are disclosed. A method for the reduction of melanin distribution, and the composition thereof to reduce melanin distribution are disclosed. A representative composition comprises 4-ethoxybenzaldehyde and one or more additional active agents as well as a pharmaceutically acceptable carrier or excipient. Carriers and excipients may be formulated for topical administration. Compositions may also be formulated for transdermal administration. The compositions may be used for the prevention and treatment of pigmentation disorders, by way of non-limited example, post-inflammatory hyperpigmentation and others. The compositions may be used for lightening skin.
US20110046100 Texaphyrin solutions and pharmaceutical formulations A packaging system is described for a drug that provides protection from contamination, crystallization and/or degradation of the drug during storage of the system prior to its use. The packaging of the drug does not significantly absorb, react with, or otherwise adversely affect the therapeutic effectiveness of the drug or other excipients or components during storage of the system prior to its use. The packaging system is also used for preserving a drug, particularly a drug containing high-purity texaphyrin metal complexes, by providing a product packaging system that prevents, limits or otherwise controls degradation reactions that can result from exposure to oxygen and/or light.
WO2008152471A1 Quinazoline derivative useful as toll-like receptor antagonist Compound CPG 52364 having formula (I) and pharmaceutically acceptable salts thereof are inhibitors of signaling by Toll-like receptors TLR7, TLR8, and TLR9, and they are useful in treatment of unwanted Immune activity. Pharmaceutical composition including CPG 52364 or a pharmaceutically acceptable salt thereof is provided and can be used to treat conditions including autoimmune disease, transplant rejection, graft- versus-host disease, allergy, asthma, sepsis, and other inflammatory conditions.
CN102920824A Liniment for treating bedsore and preparation method thereof The invention relates to liniment for treating bedsore, which is prepared by using Chinese and Western medicaments as raw material drugs. The liniment is prepared by a method comprising the following steps: grinding selected golden thread, golden cypress, common cephalanoplos herb, tribulusterrestris and lightyellow sophora root into powder of 100-120 meshes; immersing for one week with purified water; filtering to obtain filtrate 1; adding 10g of chloramphenicol into the filtrate 1; and sterilizing and disinfecting to obtain the liniment product. The liniment consisting of Chinese and Western medicaments has the functions of inhibiting bacteria and sterilizing, and promoting blood circulation to remove stasis, and can achieve the bedsore treatment aims of quick response and no relapse.
WO2008020606A1 Antiangiogenic agent An antiangiogenic agent comprising an indazole derivative represented by the formula (I) [wherein R1 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group] or a pharmacologically acceptable salt thereof as an active ingredient; an inhibitor of a kinase involved in angiogenesis, comprising an indazole derivative represented by the formula (I) or a pharmacologically acceptable salt thereof as an active ingredient; a therapeutic agent for a disease associated with angiogenesis, comprising an indazole derivative represented by the formula (I) or a pharmacologically acceptable salt thereof as an active ingredient. (I)
US20110319423 Novel dopamine d3 receptor ligands and preparation and medical uses of the same The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.
CN1868463A Slow-release prepn. contg. alpha-lipoic acid or its derivatives, and preparing method therefor A slow-release tablet of alpha-thioctic acid or its derivative used as medicine, food additive, or cosmetic has a single slow-release layer made of hydroxypropyl methylcellulose or one slow-release layer plus one ordinary-release layer for quickly releasing the alpha-thioctic acid or its derivative. Its preparing process is also disclosed.
CN102198097A Emulsion type nasal spray containing ciclesonide, and application thereof The invention relates to an emulsion type nasal spray containing ciclesonide, and an application thereof, in particular to an emulsion type nasal spray prepared from ciclesonide and pharmaceutically acceptable solvents or surfactants, and an application thereof. The emulsion type nasal spray is prepared from ciclesonide as an active component and pharmaceutically acceptable auxiliary materials by a certain preparation process, and can be used for treating asthma, allergic rhinitis and chronic obstructive pulmonary disease. In the invention, ciclesonide is used as an active component and some specific kinds and proportions of auxiliary materials are added to develop the emulsion type nasal spray according to the preparation process specified by the invention, and the dosage form has very ideal physical and chemical stabilities and excellent administration characteristics.
CN102488692A Application of AHAS (acetohydroxyacid synthase) inhibitor compound in preparing antifungal medicament The invention relates to an application of an AHAS (acetohydroxyacid synthase) inhibitor in preparing a medical antifungal medicament, and mainly relates to an application of sulfonylurea compounds (chlorimuron ethyl, ethoxysulfuron, bensulfuron methyl and pyrazosulfuron ethyl) in preparing medicaments capable of resisting Candida albicans, Cryptococcus neoformans, Saccharomyces cerevisiae, Candida parapsilopis and Candida glabrata and the like. The compounds can be used for intensely restraining the AHAS from fungal, and has a higher restraint effect on multiple types of fungi capable of causing infection at the cellular level.
US7193108 Phenylpropionic acid derivatives Specified phenylpropionic acid derivatives and analogues thereof have an antagonistic activity to α 4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α 4 integrin, such as inflammatory diseases in which α 4 integrin-depending adhesion process participates in the pathology, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.
CN101884613A Moxifloxacinhydrochloride sodium chloride injection, preparation method thereof and use thereof The invention relates to moxifloxacinhydrochloride sodium chloride injection. The injection comprises the following components in percentage by weight/volume: 0.03 to 1 percent of moxifloxacinhydrochloride, 0.01 to 3 percent of weak acid, 0.01 to 3 percent of salt of weak acid, 0.01 to 3 percent of phosphoric acid, 0.01 to 3 percent of amino acid or phosphate and 0.65 to 0.95 percent of sodium chloride.
US20060009497 Novel tetrahydropyridine derivatives as renin inhibitors The invention relates to novel tetrahydropyridine derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
US7790749 Antiulcer agents; gastrointestinal disorders; anticancer agents; anemia A method of preventing or treating diseases mediated by Helicobacter pylori, comprising administering to a subject in need of such treatment an effective amount of pleuromutilin.
US8101793 Retinoid derivatives with antiangiogenic, antitumoral and proapoptotic activities Are described compounds of Formula (I) in which R, R′, R″, A, and D have the meanings described in the text, as useful agents in the cure of pathologies characterized by altered angiogenesis and as antitumorals.
US20120178697 Compositions and methods for the inhibition of dishevelled proteins The Wnt signaling pathways are involved in embryo development as well as in tumorigenesis. Dishevelled (Dvl) tranduces Wnt signals from the receptor Frizzled (Fz) to downstream components in canonical and non-canonical Wnt signaling pathways, and the Dvl PDZ domain plays an essential role in both pathways, and the Dvl PDZ domain binds directly to Fz receptors. In the present invention using NMR-assisted virtual ligand screening, several compounds were identified and were found to bind to the Dvl PDZ domain. Molecular dynamics simulation was used to analyze the binding between the PDZ domain and these compounds in detail. These compounds provide a basis for rational design of high-affinity inhibitors of the PDZ domain, which can block Wnt signaling by interrupting the Fz-Dvl interaction.
WO2012177075A2 Composition containing antibiotics and lysophosphatidylcholine for boosting immunity or treatment of bacterial infections The present invention relates to: a pharmaceutical composition containing lysophosphatidylcholine or analogs thereof and antibiotics as active ingredients for boosting immunity or the treatment of bacterial infections; a method for boosting immunity or the treatment of bacterial infections, which comprises a step for administering the composition; and a kit containing the composition for boosting immunity or the treatment of bacterial infections.
EP1553947A2 Quinazolinones and derivatives thereof as factor xa inhibitors The present application describes quinazolinones and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
WO2014093869A1 6-substituted quinazolinone inhibitors The present technology relates to compounds and compositions of Formulas I-III and methods using such compounds. The compounds and compositions described herein may be used in the treatment or prophylaxis of diseases associated with an alphavirus, for example, Venezuelan equine encephalitis virus (VEEV).
WO2011016814A1 5α-ANDROSTANE-3,6,17-TRIONE (KNELLER'S TRIONE) AND METHODS OF USE THEREFOR Disclosed are compounds such as 5α-androstane-3, 6, 17- trione, formulations comprising said compounds, and methods of use thereof to stimulate endogenous testosterone production and improve athletic performance and libido.
EP1997506A1 Use of ck2 inhibitor for the treatment and chemosensibilization of refractory tumors to anticancer drugs This invention is related to a pharmaceutical combination that contains a Casein kinase 2 (CK2) peptide inhibitor (termed P15) along with the standard chemotherapeutic drugs used in cancer treatment and which are administered together, separated or sequentially. The chemothearapeutic drugs include cisplatin, taxol, alkaloids from Vinca, 5-fluorouracil, doxorubicin, cyclophosphamide, etoposide, mitomicin C, imatinib, iressa and velcade (vortezomib). The synergism between the P15 peptide and the anticancer drugs achieves an efficient concentration of each cytostatic drug in the combination which is from 10- to 100-fold lower than that for each cytostatic drug alone. The pharmaceutical combination described in this invention exhibits lower toxicity compared to that reported by the anticancer therapeutics and therefore, it represents a crucial advantage for its use in cancer therapy. Furthermore, the sequential administration of this pharmaceutical combination through the pretreatment with the P15 peptide leads to the chemo sensibilization of refractory tumors to the anticancer therapeutics.
EP1740568A2 Benzofuran and benzothiophene derivatives useful for the treatment of cardiovascular disease. A compound of formula (I) and pharmaceutically acceptable salts and solvates and hydrolysable esters thereof, where X, X1, X2, X3, X4 and R, R2, R3, R4 are defined as in claim 1. These compounds are activators of the hPPAR receptors and are useful for the treatment of cardiovascular disease.
CN103156861A Application of oleanolic acid derivative and pharmaceutically acceptable salts thereof in diabetic eye disease treatment The present invention discloses an application of an oleanolic acid derivative and pharmaceutically acceptable salts thereof in diabetic eye disease treatment. The oleanolic acid derivative is prepared into a nanometer preparation, a microsphere preparation and a hydrogel by using a polymer, such that toxicity of the oleanolic acid derivative is substantially reduced, an administered dose is increased, the obtained drug can provide an effect in eyes, and can provide stronger therapeutic effects compared to ordinary preparations and other long-acting preparations of the oleanolic acid derivative, the effect can be lasted for a plurality of months, and is uniform, and the drug can provide treatment effects for various or most of diabetic eye diseases, and can be taken at the diabetic eye disease initial stage so as to relieve patient pain, such that pathogenetic condition deterioration can be avoided, and surgeries and other surgical treatment methods with heavy traumas can be avoided.
WO2014044399A1 New spiroepoxide tetrahydrobenzotriazoles and their use as metap-ii inhibitors The present invention relates to new spiroepoxide tetrahydrobenzotriazole compounds, a method for their production and their use as MetAP-II inhibitors, which are particularly useful as inhibitors of angiogenesis. The compounds are characterized by formula (I) R1 = OC(O)R2 where R2 is alkyl, cycloalkyl, aryl, heteroaryl, or cinnamyl or R1 = OC(0)NHR3 where R3 is alkyl, cycloalkyl, aryl, or heteroaryl or R1 = NHC(0)OR4 where R4 is alkyl or R1 = OH, NH2 R5 = alkyl, cycloalkyl, CH2R6 where R6 is aryl or heteroaryl
US20100173885 Organometeallic compounds The present invention relates to novel organometallic compounds for use as a medicine, in particular in photodynamic therapy against various diseases, such as cancer or inflammatory and/or immune disorders. The compounds comprise a central porphyrin or phtalocyanine backbone to which ligand linkers coordinated to at least one transition metal are attached. Eta-5 or eta-6 arenes further bind to the transition metal. According to a preferred embodiment, the compound is a tetranuclear Ruthenium (+II) complex.
WO2007017901A3 Silver nanoparticle dispersion formulation A topical semisolid (gel) formulation of nanoparticles of silver and the method for producing improved topical semisolid (gel) formulation. The topical formulation comprises about 0.001% w/w to about 1% w/w of silver by weight of the total mass of the formulation with its particle size in the range of 0.1 to 150 nanometer; about 0.5% w/w to about 25% w/w of at least one gel forming agent by weight of the total mass of the formulation; about 25% w/w to 60% w/w of at least of one co-solvent by weight of the total mass of the formulation; about 1% w/w to 50% w/w of purified water by weight of the total mass of the formulation and other optional adjuvants. The nanoparticle size of the silver is responsible for the enhanced therapeutic action of the formulation.
CN103524392A Azetidines as mek inhibitors for the treatment of proliferative diseases Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
US20100111972 Method for preventing or treating opiate tolerance and dependence The present invention provides a method for preventing or treating opiate tolerance and dependence by administering to an individual in need of such treatment with a pharmaceutically effective amount of a blocking reagent for ephrinB-EphB signaling. The opiate tolerance and dependence can be caused by chronic morphine treatment and withdrawal. The blocking reagent can be an EphB receptor blocker such as EphB1-Fc and EphB2-Fc.
EP1274687B1 1,2,3,4- tetrahydroisoquinoline derivatives The invention relates to novel 1,2,3,4-tetrahydroisochinoline derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
EP1539113A2 Modified release ketoprofen dosage form The present invention relates to a modified release pharmaceutical composition of ketoprofen which comprises uncoated pellets designed to an immediate release of ketoprofen, and coated pellets release designed to a delayed and prolonged release. This composition is suitable for twice daily administration.
US20110274638 Oxoazetidine derivatives, process for the preparation thereof and use thereon in human medicine and in cosmetics Compounds derived from oxoazetidine corresponding to general formula (I) compositions containing same, processes for their preparation and their use in pharmaceutical or cosmetic compositions are described.
US20080008744 Novel tissue support The present disclosure provides tissue supports which may be utilized by themselves or in combination with other tissue closure means to enhance wound closure and healing. The tissue supports are made of a material which shrinks upon application of heat or light to further support the tissue and/or wound to which it is applied.
US7973015 Induction of exon skipping in eukaryotic cells The present invention provides a method for at least in part decreasing the production of an aberrant protein in a cell, the cell comprising pre-mRNA comprising exons coding for the protein, by inducing so-called exon skipping in the cell. Exon-skipping results in mature MRNA that does not contain the skipped exon, which leads to an altered product of the exon codes for amino acids. Exon skipping is performed by providing a cell with an agent capable of specifically inhibiting an exon inclusion signal, for instance, an exon recognition sequence, of the exon. The exon inclusion signal can be interfered with by a nucleic acid comprising complementarity to a part of the exon. The nucleic acid, which is also herewith provided, can be used for the preparation of a medicament, for instance, for the treatment of an inherited disease.
WO2010024298A1 Potassium channel regulator Disclosed is a compound represented by formula (I) [wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the description] or a pharmaceutically acceptable salt or solvate thereof.
CN102091031A Preparation method of arylhydroxamic acid organotin anti-tumor compound injection The invention belongs to the field of pharmaceutical preparations, and relates to a preparation method of an arylhydroxamic acid organotin anti-tumor compound injection. The invention solves the problems of poor dissolvability and low bioavailability of the compounds. The preparation method comprises the following steps: under clean conditions, sequentially adding 20-80% of alcohols capable of being used as injection solvents, 0.25-1% of organic bases capable of being used as injection solvents and the balance of normal saline, and uniformly mixing to obtain a ternary injection solvent; accurately weighing arylhydroxamic acid organotin anti-tumor compounds according to a prescription; adding the ternary injection solvent; stirring until the compounds are fully dissolved; filtering; encapsulating; and sterilizing to obtain the injection of the compounds, wherein the medicament concentration is 3mg/ml. By adopting the injection for direct administration, the bioavailability of the injection can be greatly improved. The preparation method is simple, convenient and economical and is suitable for popularization and application.
US20110105488 Substituted pyrrolidine and piperidine compounds, derivatives thereof, and methods for treating pain The present application relates to pyrrolidine, piperidine, and other nitrogen-containing heterocyclic derivatives and the use of these compounds for treating and preventing pam or inflammation. The analgesic compounds demonstrate efficacy in the treatment of neuropathic pain resulting from a variety of conditions such as diabetic neuropathy, HIV infections, and post-herpetic neuralgia.
CN101778846B 1,2-diamido-ethylene derivatives as orexin antagonists The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) NHNR 3 OAOR 1 R 2 (I) wherein R1, R 2, R 3, and A are as described in the description and their use as medicaments, especially as orexin receptor antagonists.
WO2011040432A1 Eye wash agent Disclosed is an eye wash agent including a carboxyvinyl polymer and a monoterpene. The amount of eye wash agent used each time is 500 µL or more. Further disclosed are an eye wash agent for washing away makeup and an eye wash agent for washing away pollen, both eye wash agents comprising a carboxyvinyl polymer and a monoterpene.
US20120141576 Treatment of Dermatologic Skin Disorders Retinal and its derivatives are incorporated with liposomes in therapeutic compositions for topical application to prevent or alleviate the conditions and symptoms of cosmetic and dermatologic disorders are described as follows. In particular, retinal and its derivatives are combined with liposomes to increase the penetration of the retinal into the skin, to provide hydration of the skin during treatment, to reduce irritation of the skin during the application of the retinal, for use as a chemical skin peel and other embodiments and uses. The present invention includes utilizing retinol products, and particularly retinal in combination with liposomes each of these embodiments and uses separately as well as in combinations with one another.
WO2007048332A1 A pharmaceutical composition for treating gout and its preparation and use A pharmaceutical composition for treating gout and its application in preparation of medicines for treating gout are provided. The said pharmaceutical composition comprises effective amount of febuxostat or its pharmaceutical salts or its solvates and a uric acid eliminant.
EP1744752A2 A method for the prevention of thromboembolic disorders The present invention relates to a method for the prevention of thrombotic, embolic and/or hemorrhagic disorders, such as cerebral infarction (stroke) or myocardial infarction, by administering levosimendan or its metabolite (II) or any of their pharmaceutically acceptable salts to a mammal in need of such prevention.
US20120094995 2-aza-bicyclo[2.2.1]heptane compounds and uses thereof This invention relates to 2-aza-bicyclo[2.2.1]heptane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating the glycine transporter 1 (GlyT1) and for the treatment of psychosis, cognitive disorders, bipolar disorders, depression disorders, anxiety disorders, post-traumatic stress disorders and pain.
CN102050792A 2-[(substituted phenylamino) carboxyl methylmercapto]-6-aryl-3H-pyrimidine-4-ketone derivative as well as preparation method and application thereof The invention relates to a 2-[(substituted phenylamino) carboxyl methylmercapto]-6-aryl-3H-pyrimidine-4-ketone derivative, and in the general expression, R1 is methyl or ethyl, R2 is 4-chlorine, 4-bromine or 4-methoxyl, and Ar is alpha-menaphthyl or 2, 6-difluorobenzyloxy. The invention further discloses the preparation method of the compound and the application as an anti-influenza plant virus inhibitor.
US20120207687 Topical formulations of targeted nitroxide agents A method for preventing or treating skin damage in a radiotherapy subject, comprising topically administering to the subject a composition that includes a therapeutically effective amount at least one targeted nitroxide agent and at least one additional ingredient.
US20120015932 Pyrazole Derivatives Used as CCR4 Receptor Antagonists Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.
CN102847072A Medicine for treating systemic lupus erythematosus and preparation method thereof The invention discloses a medicine for treating systemic lupus erythematosus and a preparation method of the medicine. The medicine is mainly prepared by the ingredients such as radix curcumae, astragalus mongholicus, seed of Chinese dodder, red flower, earthworm, honeysuckle, gypsum, angelica sinensis, folium mori, golden cypress and fructus ligustri lucidi according to a certain weight proportion. The medicine provided by the invention has functions of clearing away heat and toxic materials, nourishing yin to lessen fire and invigorating blood and removing stagnate, is used for treating the systemic lupus erythematosus, and is rapid in effect taking, short in treatment course and free of relapse.
US7205307 Pyrimidines as novel openers of potassium ion channels The present invention provides a genus of pyrimidine amides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.
CN102532223A Process for the preparation of 11,12-cyclic erythromycin a carbonate lactobionate and the use thereof The invention discloses the process for the preparation of 11,12-cyclic erythromycin A carbonate lactobionate and the use thereof. The method comprises the following steps: applying the lactose acid solution to the water suspending liquid of 11,12-cyclic erythromycin A carbonate lactobionate at a temperature ranging from 2 to 15 DEG C for sustained optimization of 8 to 14 hours; and filtering the product for spraying drying and freeze drying. According to the application of the 11,12-cyclic erythromycin A carbonate lactobionate of the invention, after being dissolved in the injection-use solvent having proper size, the single dose 50 to 1000 mg (preferably 100mg to 600g) are used for preparing the injection preparation of the antibiosis treatment medicine.
EP1435947B1 2-phenyl benzimidazoles and imidazo-¬4,5|-pyridines as cds1/chk2-inhibitors and adjuvants to chemotherapy or radiation therapy in the treatment of cancer 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines of formula (I) are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer. wherein W is COOH, -(CO)NHR1, or -(SO2)NHR1 R1 is H or C1-4alkyl; Q is N or CH; Ra and Rb are H or halogen; Y, Y1 and Y2 are independently selected from N and C-Rc with the proviso that 0, 1 or 2 of Y, Y1 and Y2 are N and at least 2 of Rc must be hydrogen; Rc are independently selected from the group consiting of -H, -OH, -C1-6alkyl, -SCF3, halo, -CF3 and -OCF3; Z is selected from the group consisting of O, S, SO, SO2, SO2NR2, NR2SO2, NH, CONR2, piperazin-diyl or a covalent bond; R2 is H or C1-4alkyl; AR1 is an aromatic group as defined in the claims.
CN101129367B S-omeprazole solid dispersion and composition containing the dispersion The invention relates to a solid dispersion in medicinal field based on S-omeprazole and derivative as active ingredient and being added with carrier material to form solid dispersion, which comprises 22mg-458mg S-omeprazole per gram and can be intermediate compound of medicinal compositions. The invention is characterized by the following: the solid dispersion and the medicinal compositions can be absorbed in the intestinal canal with good bioavailability and used for diseases raised through gastric hyperacidity such as gastric ulcer. The invention has higher external dissolvability than the conventional preparation of S-omeprazole zinc and the bioavailability is homologous to 97.5% S-omeprazole magnesium intestinal dissolving tablet, which can last for longer time and provides a new choice for clinical treating the gastric ulcer.
WO2013061269A1 Combinations of loteprednol and olopatadine for the treatment of ocular allergies The present invention relates to use of a fixed dose combination comprising Loteprednol or its pharmaceutically acceptable esters/salts thereof and Olopatadine or its pharmaceutically acceptable salts thereof for the treatment of ocular allergy. The present invention further relates to a pharmaceutical composition comprising a fixed dose combination comprising Loteprednol or its pharmaceutically acceptable esters/salts thereof and Olopatadine or its pharmaceutically acceptable salts thereof for the treatment of ocular allergy.
US20100298344 Polycationic Compounds And Uses Thereof Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.
CN101041010A Medicine compound for treating diabetes and its preparation The invention provides a pharmaceutical composition for treating diabetes, which is prepared from the constituents of (by weight ratio) calcium sulphate 299 parts, anemarrhena rhizome 160 parts, dried rehmannia root 200 parts, ophiopogon root 160 parts, root of Chinese trichosannthes 239 parts, radix polygonati officinalis 200 parts, radix scrophulariae 160 parts, achyranthes and cyathula root 119 parts, radix salvia miltiorrhiza 200 parts, alisol 160 parts, root of pilose asiabell 160 parts, cornus officinalis 160 parts, loquat leaves 119 parts and schisandra fruit 99 parts.
US20080234312 Feed or Feed Additive Containing an Alkaloid The invention relates to a feed containing conventional feed substances, or feed additives for producing said feed. According to the invention, the feed or fed additive contains a protopine alkaloid, in particular α-allocryptopine, preferably in combination with at least one benzophenanthridine alkaloid in an active quantity as a stimulant and appetite enhance for commercial animals.
WO2010025906A3 Hybrid antimicrobial compounds and their use The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain antimicrobial compounds comprising pharmacophores based on or comprising benzyl pyrimidines and 4-quinolones or 4H-4-oxoquinolizines (for convenience, collectively referred to herein as "BP-4Q compounds"), which, inter alia, are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.
US20110071145 Raf Modulators And Methods Of Use The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
WO2014102593A1 Substituted morphinans and the use thereof The application is directed to compounds of Formula (I), and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4a, and R4b are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I) to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
EP1272200B1 Divided dose therapies with vascular damaging activity The invention concerns the use of a vascular damaging agent or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for administration in divided doses for use in the production of a vascular damaging effect in a warm-blooded animal such as a human. In particular the vascular damaging agent is ZD6126, or a pharmaceutically acceptable salt thereof. The invention also relates to methods of treatment using a vascular damaging agent in divided doses.
US20080107754 Dietary supplement and a method to enhance sleep and lucid dreaming A nutritional supplement for enhancing sleep and lucid dreaming in humans. It contains a combination of ingredients in proportions calculated to enhance lucid dreaming. The primary ingredients are Calea zacatechichi, L-5-Hydroxytryptophan (L-5-HTP), and Vinpocetine. In addition, the nutritional supplement may include the secondary ingredient Melatonin and the tertiary ingredients Wild Lettuce Extract, Mugwort Extract, Dimethylaminoethanol Powder (DMAE), Passionflower Extract and Green Tea Extract. Further, various Vitamins may be added such as certain B vitamins, D and C, as well as Zinc, Magnesium and Calcium. The selection and amounts of the ingredients of the nutritional supplement promotes sleep and lucid dreaming in people who have taken the nutritional supplement prior to going to sleep.
EP1492540B1 The use of devazepide as analgesic agent There is described a method of treatment of a patient requiring analgesic therapy which comprises the administration of an analgesically effective amount of devazepide. There is also described the use of devazepide in the manufacture of an analgesically effective medicament.
CN101619054B New coumarin active content, preparation method and application thereof The invention relates to a new coumarin active content, i.e. pigeon pea lactone extracted and separated from cajan leaves, an extraction and separation method and an application thereof. The structure of the compound is shown as a figure 1. The invention adopts the technical scheme that agricultural waste of cajan leaves is used as raw material which is extracted by a solvent; the extracting solution is concentrated and dispersed in water; an ultrasonic oscillation flocculation technology, a bubble column extraction technology and a column chromatography separation technology in positive-phase silica gel are adopted and combined with a low-temperature crystallization and recrystallization technology to obtain the content with the purity higher than 95 percent; and the anti-oxidation activity and the action of the chemical content on cardiovascular diseases are detected by a DPPH model, a beta-renieratene-linoleic acid model, an in-texture SOD enzyme model, a platelet aggregation modelinduced by ADP in corpora and an aorta systole model induced by phenylephrine. Results show that the active content has favorable free radical scavenging activity, anti-oxidation activity in corpora and in vitro, platelet aggregation restraining action in corpora and a certain hemangiectasis action. Meanwhile, the preparation method of the pigeon pea lactone in the invention is easy and practicaland can obtain a product with high purity high yield and high added value in a short period which is suitable for industrialized production and application, can be further developed and researched into a new antioxidant as an additive for medicines, foods and cosmetics.
EP1262555B1 Protein hollow nano particles, transporter with the use of the same and method of introducing substance into cells Hollow nano particles composed of a hepatitis B virus (HBV) surface antigen protein and a biorecognition molecule introduced thereinto which are usable as a protein capable of forming particles as a common means of specifically and safely transporting and introducing substances (gene, protein, compound, etc.) into the target cells or tissue.
US20050245765 Partially hydrolyzing methyl formates with water; forming a formic acid/water stream; reacting the methyl formate stream with a base in the presence of water; distilling off methanol; and combining the formic acid and water stream with the formate and water stream The invention relates to a method for producing formic acid formates, whereby (a) formic acid methyl ester is partially hydrolysed with water; (b) formic acid methyl ester and methanol are separated by distillation from the reaction mixture obtained in step (a), forming a current containing formic acid and water; (c) the current obtained in step (b), containing the formic acid methyl ester and optionally methanol, is converted into a current containing formate and water, by (i) reaction with a basic compound having a pKa value of the corresponding acid of the corresponding dissociation step of=3, measured at 25° C. in an aqueous solution, in the presence of water, and (ii) separation by distillation of the methanol; and (d) the current obtained in step (b), containing formic acid and water, and the current obtained in step (c), containing formate and water, are combined to form a mixture containing the formic acid formate and water. The invention also relates in a device for producing said formic acid formates and to the use of the same.
WO2009003993A1 Piperidine derivatives useful as orexin receptor antagonists This invention relates to imidazo[1,2-alpha]pyridin-2-ylmethyl substituted piperidine derivatives of formula (I) and their use as pharmaceuticals, in the treatment of obesity and diabetes.
US20080085886 Anticancer and/or antiinflammatory activity, MEK (MAP kinase kinase) inhibitors; for example, 3-(2-Fluoro-4-iodo-phenylamino)-furo[3,2-c]pyridine-2-carboxylic acid ((R)-2,3-dihydroxy-propoxy)-amide The invention relates to azabenzofuranyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzofuranyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
CN101019824A Oral medicine composition containing salvianolic acid and its prepn The present invention discloses one kind of oral medicine composition containing red sage salvianolic acid and its preparation process. The oral medicine composition has the composition determined through pharmacodynamic experiment, pharmacokinetic experiment and toxicologic experiment as red sage salvianolic acid 1-10 weight portions and breviscapine 1-20 weight portions, preferably red sage salvianolic acid 1-5 weight portions and breviscapine 1-5 weight portions. The present invention also discloses the detection and analysis method and the use of the medicine composition. Pharmacologic experiment shows its excellent pharmacologic effect.
US20120115805 Use of at least one nucleic acid to influence the natural pigmentation process A method for influencing the natural pigmentation process of skin or appendages thereof, includes the step of topically contacting the skin or appendages thereof with at least one nucleic acid containing at least 55% guanine nucleotide.
WO2009145243A1 Lipid membrane applicable to photodynamic therapy and application thereof Disclosed is a new technology to enable a substance which cannot be applied in a wavelength range preferred for photodynamic therapy to be applied in the same wavelength range. Provided is a lipid membrane containing a photosensitive substance as a donor molecule and a photoactivated substance as an acceptor molecule. Also provided is a cell proliferation inhibitor and a photodynamic therapeutic agent containing this lipid membrane.
EP0859613B1 Use of flupirtin for the prevention and treatment of diseases which are associated with damage to the haemopoietic cell system The invention relates to the use of flupirtin or the salts thereof as a drug for the prevention and treatment of diseases which are associated with damage to the haemopoietic cell system, for example lymphocytes. It is particularly important in the treatment of HIV-infected patients or AIDS patients.
WO2010087761A1 2-aza-bicyclo[2.2.2]octane compounds and uses thereof This invention relates to 2-aza-bicyclo [2.2.2] octane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating the glycine transporter 1 (GIyTl) and for the treatment of psychosis, cognitive disorders, bipolar disorders, depression disorders, anxiety disorders, posttraumatic stress disorders and pain.
US20090155338 Chronotherapeutic Ocular Delivery System Comprising a Combination of Prostaglandin and a Beta-Blocker for Treating Primary Glaucoma Chronotherapeutic delivery system for treating primary open-angle glaucoma, comprising a delivery system incorporating pharmaceutical products for delivery to an eye in the treatment of primary open-angle glaucoma (POAG), comprising: (a) a biocompatible erodible material incorporating a therapeutically-effective amount of a prostaglandin analogue, and (b) a reservoir containing a therapeutically-effective amount of a beta-blocker, whereby, when the delivery system is placed in the eye the prostaglandin analogue is delivered gradually as the erodible material is eroded, and the beta-blocker is delivered rapidly when at least a predetermined portion of the erodible material has been eroded.
WO2013082548A1 Oligonucleotides for treating expanded repeat diseases The invention provides for a method for selectively reducing the expression of a mutant mRNA and/or protein having an expanded nucleotide repeat relative to a wild-type mRNA, comprising contacting a cell with an antisense oligonucleotide of sufficient length and complementarity to the expanded nucleotide repeat. More particularly it relates to selectively reducing the expression of mutant Huntington protein associated with Huntington's disease. The antisense oligonucleotide comprising either a nucleotide or a repeated three nucleotide sequence as defined in the claims.
US20070232580 Novel sterol/stanol nitroderivatives and use thereof in treating or preventing cardiovascular disease, its underlying conditions and other disorders Sterol and stanol nitro derivatives and their use in treating or preventing cardiovascular disease, its underlying conditions and other disorders are disclosed. The disclosed nitro derivatives are synthesized by ester linkage of a nitric oxide (NO)-releasing moiety to a sterol or stanol compound.
US20120022149 Pharmaceutical composition with enhanced solubility characteristics There are disclosed pharmaceutical compositions, particularly ophthalmic compositions, that contain relatively high concentrations of solubility enhancing polymer (e.g., polyether polymer, polyvinyl polymer or a combination thereof) for providing enhanced solubility of one or more therapeutic agents. In a preferred embodiment, the composition is a multi-dose topical aqueous ophthalmic composition that contains relatively high concentrations of solubility enhancing polymer (e.g., polyether polymer, polyvinyl polymer or a combination thereof) for providing enhanced solubility of one or more therapeutic agents.
US20080187576 Osteoarthritis; rheumatic diseases; gene therapy; interleukin receptor antagonist peptide or polypeptide Disclosed are methods and compositions for treating articular diseases such as osteoarthritis and rheumatoid arthritis, or articular dysfunction in mammals. Also disclosed are self-complimentary AAV vectors useful in gene therapy and delivery of therapeutic constructs to mammalian cells, and in particular, articular joints, cartilage, ligaments, tendons, and surrounding tissues.
CN102885780A Method for improving bioavailability of resveratrol The invention relates a method for improving bioavailability of resveratrol. The method is simple and convenient and can be operated easily. The method overcomes the defects of the prior art and adopts a modern pellet-forming technology. Through deep analysis of physical and chemical properties of resveratrol, based on a dissolution rate as an index, an excipient and a binder as medicinal auxiliary materials are determined by scientific tests. The method utilizes a small amount of the auxiliary materials, has stable quality, good effect reproducibility, and a low adverse reaction occurrence rate. Pellets obtained by the method can be distributed on a large area of the surface of an absorption organ so that human relative bioavailability F is improved to 85.42% from 76.75% and local stimulation is reduced and more choices are provided for consumers.
CN101845021A Quinazoline ketones alkaloid and preparation method and application thereof The invention relates to quinazoline ketones alkaloid and a preparation method and application thereof; in the invention, separation is carried out in a sea mud sample from offshore Baima Jingzhen in Danzhou in Hainan to obtain bacterium-Baxillus ereus 041381, and the compounds with novel structure are produced by the bacteria with culture preservation number CCTCC M 203030, and the compounds are prepared by a chemical synthesis method; proved by experiments, the compounds have candida albicans resisting activity, the minimum inhibition concentration MIC is 1.3-10.2mum, therefore, the compounds can be used as inhibitors of candida albicans.
WO2012033144A1 Pyrazoloquinoline compound [Problem] To provide a compound that has PDE9-inhibiting activity and is useful as an active ingredient of an agent for treating and/or preventing overactive bladder, dysuria, bladder and urinary tract disease, and the like. [Solution] The inventors of the present invention studied compounds that have PDE9-inhibiting activity and are useful as active ingredients of agents for treating and/or preventing overactive bladder, dysuria, bladder and urinary tract disease, and the like, and perfected the present invention upon confirming that pyrazoloquinoline compounds have PDE9-inhibiting activity. The pyrazoloquinoline compound of the present invention has PDE9-inhibiting activity and can be used as an agent for preventing and/or treating overactive bladder, dysuria, bladder and urinary tract disease, and the like.
US7226596 Metalloenzymes; antiproliferative agents; anticarcinogenic agents; cancer diagnosis; antisense agents; complementary determining regions The invention concerns compositions and methods for the diagnosis and treatment of neoplastic cell growth and proliferation in mammals, including humans. The invention is based upon the identification of an ADAM8 gene that is amplified in the genome of tumor cells. Such gene amplification is associated with the overexpression of the gene product as compared to normal cells of the same tissue type and contributes to tumorigenesis. Accordingly, the ADAM8 protein encoded by the amplified gene is a useful target for the diagnosis and/or treatment (including prevention) of certain cancers, and acts as a predictor of the prognosis of tumor treatment.
EP1900360A1 Homer a new target of treating psychiatric disorders A method for treatment of psychosis, schizophrenia, oncological disorders, tumors and/or CNS disorders in a human being comprising administering to said human being a composition comprising an effective amount of a compound which interacts with homer or metabotropic receptors are disclosed.
CN101209248A Preparation of tamoxifen citrate microcapsule prepared by complex coacervation method The invention relates to a complex coacervation method for preparing the tamoxifen citrate microcapsule, the steps include: (1) the capsule core tamoxifen citrate is weighed and dissolved in 95 percent of ethanol for ultrasonic dissolution, Arab gum solution is added, the mixture is treated ultrasonically in a water bath, then the gel water solution is added, and the water bathing and stirring are carried out to control the weight ratio of the capsule core and the capsule material; (2) 10 percent of glacial acetic acid is added to adjust the pH value to 4.0 to 4.3 during the stirring process, distilled water is added for dilution, the high-speed stirring is carried out, then the mixture is arranged in an ice bath for rapid temperature-decreasing to 0 to 10 DEG C, and crosslinker is added for curing; (3) 20 percent of NaOH solution is used for adjusting the pH value, the high-speed stirring is carried out at 0 to 10 DEG C, and the tamoxifen citrate microcapsule can be obtained by curing, centrifugalizing, washing, freezing, decompression and drying. The method is simple, safe and good in reproducibility, and the prepared microcapsule is proved to have the better sustained-release function by transdermal and in vitro dissolution results, so the invention can be taken as the drug sustained-release formulation for the prevention and treatment of breast cancer.
CN103505737A Method for preparing docetaxel/beta-cyclodextrin clathrates The invention discloses a method for preparing docetaxel/beta-cyclodextrin clathrates by a supercritical carbon dioxide fluid. The docetaxel/beta-cyclodextrin clathrates with different clathration rates can be synthesized by changing preparation pressure. Compared with the a general solution-stirring method for preparing the docetaxel/beta-cyclodextrin clathrates, the method prepared by the invention, by regulating and controlling the temperature and pressure of the supercritical carbon dioxide fluid, substantially raises the clathration rates of the docetaxel in the docetaxel/beta-cyclodextrin clathrates. Furthermore, the solubility of the docetaxel/beta-cyclodextrin clathrates prepared by the supercritical carbon dioxide method in water is higher than that of the docetaxel/beta-cyclodextrin clathrates prepared by the general solution-stirring method.
CN102232926A Oral taxol nanoparticles and preparation method thereof The invention discloses oral taxol nanoparticles, which comprise the following raw material components: taxol, poly (lactide-co-glycolide) (PLGA), a surfactant, a membrane modifying material and a drying protective agent. The taxol nanoparticles have a structure that: the taxol is wrapped by PLGA; the surfactant and the membrane modifying material are coated on the surface of the PLGA; and the drying protective agent is added and nanoparticle powder is obtained by drying. The invention also discloses the preparation method of the taxol nanoparticles. In the invention, the particle sizes of the oral taxol nanoparticles are small and uniform; after the oral taxol nanoparticles are freeze-dried or spray-dried, the particle sizes are not changed obviously; and r being taken by oral administration, the bioavailability of the oral administration of the taxol is improved considerably, and the toxic and side effects of the taxol on the whole body are reduced. The preparation method disclosed by the invention can be implemented under a condition that the taxol is stable and prevent medicine effect from lowering and can be used in industrial production.
WO2006060898A1 Method for treating inflammatory disorders The invention features a method of treating an inflammatory disorder, such as sepsis, in a subject. The method involves administering to the subject an antagonist of clAP2 expression and/or function, so that the disorder is treated.
US8367100 Preparation and use of sleeve and micro-encapsulated topical analgesic patch for treating pain Novel micro-encapsulated topical analgesics are provided to treat pain and may be applied via sleeves having dosed therapeutic sections, especially to joints and extremities. Sleeves may be prepared and packaged inside-out and inverted when positioned by the wearer.
WO2013001030A1 Oxazetidine derivatives, process for preparing them and use thereof in human medicine and in cosmetics The present invention relates to the pharmaceutical field and in particular to the treatment of hypopigmentary pathologies and photosensitive dermatoses. More specifically, the invention relates to compounds that are agonists of the MC1R receptor and which exhibit reduced toxicity relative to the other compounds of the same class. These compounds have the general formula (I) below: in which: R1 represents a cyclopropylmethyl or a 4-hydroxybutyl group; R2 represents a hydrogen atom or a methyl group; and also the salts and enantiomers of the corresponding compounds of general formula (I).
US20110039922 18beta-GLYCYRRHETINIC ACID DERIVATIVES AND SYNTHETIC METHOD THEREOF The present invention provides a chemical compound having the structure being one selected from a group consisting of wherein R1 is one selected from a group consisting of COOCH3, COOCH2Ph, CONHCH(CH3)2 and CONHC6H5, R2 is one selected from a group consisting of H, CH3 and CH(CH3)2, R3 is one selected from a group consisting of H, CH3, CH(CH3)2 and CH2Ph, and R4 is one of CH(CH3)2 and C6H5.
WO2007089166A1 Medicinal preparation for jugulating a systemic inflammatory response syndrome The invention relates to medicine and can be used in cardiology, anesthesiology and reanimation, gynecology and endocrinology. The inventive medicinal preparation, which is used for jugulating a systemic inflammatory response syndrome, comprises a cytokine hyperproduction inhibitor in the form of purine or the derivative thereof and an ADP ribosylation regulator in the form of a diphosphopyridine nucleotide. In the preferred embodiment, the purine derivative is embodied in the form of inosine. Said medicinal preparation can also contain an antibiotic, preferably gentamicine or angiotensin-converting enzyme, preferably lisinopril or a cardiac glycoside, preferably digoxin, when necessary in combination with bioflavonoid and L-acetylcarnitine. Said medicinal preparation can be embodied in the form of tablets or injections. The medicinal preparation exhibits the capacity of jugulating a systemic inflammatory response syndrome independently of the aetiology thereof and makes it possible to obtain an expressed and stable short-term therapeutic effect .
DE102004002351A1 New RNA aptamers specific for lipopolysaccharide-binding protein, useful for diagnosis and treatment of sepsis, inhibit the lipopolysaccharide-induced signaling cascade RNA aptamers (I), or their alleles and/or derivatives, that bind specifically to lipopolysaccharide-binding protein (LBP) are new. - An INDEPENDENT CLAIM is also included for a method for preparing and/or isolating (I). - ACTIVITY - Antibacterial; Immunosuppressive. No details of tests for these activities are given. - MECHANISM OF ACTION - Inhibition of LBP, a key component in the lipopolysaccharide-induced signaling cascade.
WO2012047131A1 Anti-viral agent against influenza b The invention relates to the field of medicine, more specifically pharmacology and the creation of drugs, and can be used for treating influenza caused by influenza B viruses. An anti-viral agent against influenza B is proposed which comprises 1-{[6-bromine-1-methly-5-methoxy-2-phenylthiomethyl-1-n-indole-3-yl] carbonyl}-4-benzyl-piperazine hydrochloride.
US7202267 Acyloxypyrrolidine derivatives, preparation thereof and application thereof in therapeutic The invention relates to acyloxypyrrolidine derivatives of general formula (I): in which: R1 represents a hydrogen atom, a (C1–C6)alkyl, a (C3–C6)cycloalkyl, a group —CH2CH2COOH or a group —NR2R3; R2 and R3 each represent, independently, a hydrogen atom or a (C1–C6)alkyl. Also disclosed and claimed are the method of preparation of the compounds of the invention and their application in therapeutics.
US20100056425 Absorption enhancers such as E.G. BHT, BHA or propyl gallate The invention provides a pharmaceutical composition comprising a mixture of (a) an active macromolecular principle, and (b) an aromatic alcohol absorption enhancer chosen from butylated hydroxy toluene, butylated hydroxy anisole and analogues and derivatives thereof, wherein the aromatic alcohol absorption enhancer is present in an amount by weight greater than or equal to that of the active macromolecular principle, and further comprises a pharmaceutical composition comprising a mixture of (a) an active macromolecular principle, (b) an aromatic alcohol absorption enhancer chosen from propyl gallate, butylated hydroxy toluene, butylated hydroxy anisole and analogues and derivatives thereof, wherein the aromatic alcohol absorption enhancer is present in an amount by weight greater than or equal to that of the active macromolecular principle, and (c) a solubilisation aid capable of increasing the solubility of the aromatic alcohol absorption enhancer in aqueous media.
US20100081612 Polypeptide derivatives of parathyroid hormone (pth) The present invention is related to novel parathyroid hormone polypeptide derivatives, and to pharmaceutical composition containing the polypeptides, as well as synthetic and recombinant methods for producing the polypeptides. Also disclosed are methods for treating mammalian conditions characterized by decreases in bone mass using therapeutically effective pharmaceutical compositions containing the polypeptides of the present invention. The present invention further provides diagnostic and therapeutic methods using the polypeptide derivatives.
CN102579500A Compound cod-liver oil ointment as well as preparation method and application thereof The invention relates to a compound cod-liver oil ointment as well as a preparation method and application thereof. The compound cod-liver oil ointment comprises the following raw materials in parts by weight: 80-120 parts of cod-liver oil, 35-65 parts of zinc oxide and 3.5-6.5 parts of ethacridine lactate. The compound cod-liver oil ointment has the effects of removing necrotic tissue, promoting granulation, converging, diminishing inflammation, reliving itching, clearing heat and reliving pain and promoting wound healing and has obvious curative effects of treating skin mucosa ulcer and sufferings and red swollen crissum. As a whole, the compound cod-liver oil ointment has the advantages that the curative effect is definite, use is convenient, acting is quick and the like, and is safe; no pain is generated; and the effective rate of the compound cod-liver oil ointment reaches 100%.
WO2011012868A1 Compounds for treatment of inflammation The present invention relates to the use of benzylideneaminoguanidines for the treatment of inflammation and pain. In one preferred embodiment, the invention relates to the use of N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine for the treatment of rheumatoid arthritis.
US8629156 Tryptophan hydroxylase inhibitors Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders:
US20080064717 Type 2 diabetes, obesity, elevated plasma triglycerides, metabolic syndrome, non-alcoholic steatohepatitis, and non-alcoholic fatty liver disease; N-(3-chlorophenyl)-N'-(4'-{(R)-hydroxy[(1R,2R)-2-(hydroxymethyl)cyclopentyl]methyl}-1,1'-biphenyl-4-yl)urea The present invention relates to compounds of formula (I): wherein R1, R3, X, Q, Z, A, 9, m, and n are defined herein Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
EP1337247B1 Use of Gaboxadol for the treatment of premenstrual disorder, postnatal depression or postmenopausal related dysphoric disorder The invention provides the use of a non-steroid compound which act on the GABA receptor for the treatment of disorders relating to reduced neurosteroid activity. The non-steroid compounds may be GABA agonists, GABA uptake inhibitors or enhancers of GABAergic activity.
WO2008062574A1 Sugar derivative and use thereof A sugar derivative which is derived from Aphanothece sacrum, has an average molecular weight of 2,000,000 or more, has a repeat structure of a sugar chain unit having monosaccharide structures of a hexose structurea and a pentose structure linked to one another in a linear or branched form, contains a lactated sulfated sugar, and in which 2.7 or more hydroxyl groups per 100 hydroxyl groups are sulfated, or a sulfur element is contained at 1.5% by weight or more of the total elements. This provides a useful sugar derivative which is derived from Aphanothece sacrum and has a novel polysaccharide structure.
WO2011113895A3 Characterization and validation of inhibitors and ligands of dipeptidyl aminopeptidase iv (dp iv) The invention relates to a method for characterization and validation of inhibitors or ligands of DPIV, DP8 or DP9 by their interaction with specific binding sites in silico and in vitro. It describes the use of special binding properties at the binding site of the DPIV in the central pore of DPIV, which is distant from the catalytic domain by at least 10 Angström (1 nm) which is essential for the steric inhibition of this peptidase and related enzymes like DP8 and DP9 by DPIV ligands or steric inhibitors for the use of these compounds to suppress DNA synthesis of lymphocytes, dermal cells and other cells. This finding is also important in that this technique can be used to predict unwanted side effects of DPIV related drugs and exclude effects of DPIV inhibitors developed for the treatment of Diabetes mellitus type II on immune functions and vice versa.
WO2009092720A1 4-phenyl-piperazin-1-yl-alkyl-benzoimidazol-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors This invention relates to novel 4-phenyl-piperazin-1-yl-alkyl-benzoimidazol-2- one derivatives of structure (I) useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.
WO2008108988A1 Antimicrobial heterocyclic compounds for treatment of bacterial infections The present invention provides heterocyclic compounds of the following formula (I) : or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
CN102731590A Coumarin glucoside, preparation method and application of coumarin glucoside The invention discloses coumarin glucoside, a preparation method and an application of the coumarin glucoside. Coumarin glucoside has a structural formula described in formula (I), and the coumarin oumarin glucoside with anti-fouler larva attaching activity and anti-tumour activity, which is described in the formula (I), can be separated and prepared in a boiling tube. The coumarin glucoside can be used for preparing anti-fouler larva attaching drugs and anti-tumour drugs, provides a lead compound for preparing anti-fouler larva attaching drugs and anti-tumour drugs and has wide application prospect. The formula (I) is shown in the description.
US20060062788 Method for determining MIF content The present invention relates to diagnostic methods for determining migration inhibitory factor (MIF) mRNA content in a sample, wherein MIF is human MIF polypeptide having a molecular weight of approximately 12.5 kDa and kits for detecting MIF.
US7056944 Pyrazole compositions useful as inhibitors of erk Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
US20090016963 Genes involved in neurodegenerative conditions The invention discloses suitable gene and polypeptide targets for the development of new therapeutics to treat, prevent or ameliorate neurodegenerative conditions. The invention also relates to methods to treat, prevent or ameliorate said conditions and pharmaceutical compositions therefor, as well as to a method to identify compounds with therapeutic usefulness to treat neurodegenerative conditions.
CN102008477B Method for preparing tablet drug composition containing Rosuvastatin calcium The invention relates to a method for preparing a tablet drug composition containing Rosuvastatin calcium. The preparation forms of the drug composition can be administered to the patients safely and the stability of Rosuvastatin calcium and the absorbability in gastrointestinal tract can be improved. Specifically, the invention relates to a method for preparing the drug composition containing amorphous Rosuvastatin calcium and beta-cyclodextrin. The method is characterized by grinding Rosuvastatin calcium and beta-cyclodextrin under alkaline condition, drying and crashing to obtain (80-100)-mesh fine powder, mixing the fine powder with appropriate auxiliary materials, preparing granules, carrying out tabletting and carrying out coating, thus preparing the drug composition. The in vitro release of the composition is improved to a greater degree, thus improving the bioavailability; and the composition can effectively treat hyperlipidemia, is convenient to take orally, covers the bad taste and is fast to disintegrate and absorb and convenient to carry.
US20100222387 3-Fluoro-Piperidine T-Type Calcium Channel Antagonists The present invention is directed to 3-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
WO2010134533A1 2,4-diaminopyrimidine compound having aminocyclohexylalkyl group A compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a PKCθ inhibitor, particularly as an active ingredient for a pharmaceutical composition for preventing the occurrence of an acute rejection in transplantation. (In the formula, R1 represents -H, an optionally substituted cycloalkyl group, an (optionally substituted cycloalkyl)-C1-6 alkyl group, an optionally substituted heterocycloalkyl group, or an (optionally substituted heterocycloalkyl)-C1-6 alkyl group; R2 represents -CN, -CF3, -NO2 or a halogen atom; R3 represents a halogen atom, or a -Q-(optionally substituted C1-6 alkyl) group; Q represents -O- or -S-; and A represents CH or N.)
WO2011161644A1 Treatment of hepatitis c virus related diseases using hydroxychloroquine or a combination of hydroxychloroquine and an anti-viral agent Methods of treating a hepatitis C virus (HCV) related disease are described herein, comprising administering to the subject a therapeutically effective amount of hydroxychloroquine. Therapeutically effective amounts of hydroxychloroquine are disclosed which are sufficient to inhibit HCV-induced autophagy in the subject. An anitviral agent may be co-administered with the hydroxychloroquine. Methods utilizing synergistic combinations of hydroxychloroquine and an antiviral agent are disclosed. Further disclosed are compositions comprising hydroxychloroquine and an antiviral agent, as well as hydroxychloroquine and uses thereof for the treatment of a hepatitis C virus (HCV) related disease.
US20120058180 Liver-specific Nanocapsules and Methods of Using This disclosure describes liver-specific nanocapsules for specifically targeting liver cells. This disclosure also provides methods of using such liver-specific nanocapsules to deliver one or more cargo moieties to the liver cells.
CN102631385A Compound anti-aging quercetin nanoemulsion health care product The invention discloses a compound anti-aging quercetin nanoemulsion health care product which comprises the following raw materials in mass percent: 1-15% of quercetin, 15-40% of surfactant, 1-15% of cosurfactant, 5-25% of oil, 1-15% of celery aqueous extract, 1-15% of mushroom aqueous extract, and the balance of distilled water; and the sum of mass percents of the above raw materials is 100%. The nanoemulsion is small in emulsion droplet, uniform in distribution, low in viscosity and good in liquidity. The compound anti-aging health care product takes fat soluble natural product quercetin with an efficient anti-aging effect as a main component, takes the celery aqueous extract and the mushroom aqueous extract as auxiliary components, has effects of keeping skin moisture, adjusting slumber, delaying senescence and adjusting immunologic function and has certain health care effect on diseases such as hypertension, hyperlipemia, hyperglycemia, heart disease and the like.
US20090197954 Linoleic acid preparations for the topical treatment of male and female pattern androgenetic alopecia, age-related alopecia, and keratosis pilaris A preparation for the topical application of linoleic acid to treat male and female androgenetic alopecia, age-related alopecia, and keratosis pilaris contains between about 0.1% and about 10%, preferably between about 1% and about 5%, and specifically about 2% linoleic acid by volume in its carrier vehicle. This acts to correct the local linoleic acid deficiency that exists in the follicles in these conditions and provides linoleic acid to suppress growth of Propionibacterium acnes with resultant reduction in its porphyrin production which in turn reduces microinflammation and altered keratinization that damages follicles and eliminates functioning follicles in alopecia and causes follicle plugging in keratosis pilaris.
WO2008146036A1 Combination of checkponit kinase ( chk) and telangiectasia mutated (atm) inhibitors for the treatment of cancer A combination, comprising a checkpoint kinase (CHK) inhibitor, or a pharmaceutically acceptable salt thereof, and an ataxia telangiectasia mutated (ATM) inhibitor, or a pharmaceutically acceptable salt thereof is described.
US20100303776 Methods and compositions for regulated expression of multiple nucleic acids The present invention provides a cell comprising a first heterologous nucleic acid construct and a second heterologous nucleic acid construct, wherein each of said first and second heterologous nucleic acid constructs comprises: A. a first nucleotide sequence encoding a nucleotide sequence of interest (NOI); and B. a second intronic nucleotide sequence comprising: i) a first set of splice elements defining a first intron that is removed by splicing to produce a first RNA molecule encoded by said first nucleotide sequence in the absence of activity at a second set of splice elements; and ii) the second set of splice elements defining a second intron different from said first intron, wherein said second intron is removed by splicing to produce no RNA molecule and/or to produce a second RNA molecule that is not encoded by said first nucleotide sequence, wherein each said first nucleotide sequence of each of said first and second heterologous nucleic acid constructs is different from one another and wherein each said second intronic nucleotide sequence of each of said first and second heterologous nucleic acid constructs is different from one another.
US20100021556 Method for the Production of an Agent Against an Infectious Disease A method for producing an agent against an infectious disease, particularly HIV, Ebola, or similar. In the method, a pressurized, especially medical oxygen is swirled into a solution containing at least one plant component particularly in the form of an extract.
WO2007147819A1 3h,11h-oxazolo[3',4':1,2]pyrido[3,4-b]indole derivatives and therapeutic use thereof The present invention relates to a 3H,11H-oxazolo[3',4':1,2]pyrido-[3,4-5b]indole derivative of general formula (I), in which R1 is a hydrogen atom, a C1-C6 alkyl group or a C1-C6 alkoxy group; R2 is a hydrogen atom or a C1-C6 alkyl group; the dashed line between positions 1 and 11b of the ring is absent or is a bond; R3 is a hydrogen atom, a C1-C6 alkyl group or a phenyl group, the phenyl group being optionally substituted with a halogen atom, a C1-C6 alkyl group or a C1-C6 alkoxy group, and formula (II) is formula (III) in which R4 is a hydrogen atom, a C1-C6 alkyl group or a phenyl group, the phenyl group being optionally substituted with a halogen atom, a C1-C6 alkyl group or a C1-C6 alkoxy group, or R3 is absent and formula (II) is formula (IV); or mixtures thereof, or pharmaceutically acceptable addition salts thereof, or isomers, enantiomers and diastereoisomers thereof or mixtures thereof. It also relates to a process for preparing this compound, to a pharmaceutical or cosmetic composition containing it and to the therapeutic use thereof, in particular as a hypnotic.
CN1836730A Intensified additive for chondroitin sulfate capsule formulation and tablet and its preparation method The reinforcing additive for chondroitin sulfate capsule and tablet is prepared with glucosamine hydrochloride 0.5-3 weight portions and sodium alginate 1-8 weight portions. Clinical observation proves the effect of the additive in raising the curative effect of chondroitin sulfate.
CN1915220A Mitoxantrone or liposome of mitoxantrone hydrochloric acid, and preparation method A liposome of mitoxantrone or mitoxantrone hydrochloride is prepared from mitoxantrone or mitoxantrone hydrochloride, negatively charged phosphatide, neutral phosphatide and cholate. Its preparing process is also disclosed.
US7534593 Crystals of glucokinase and methods of growing them Crystalline forms of mammalian Glucokinase, ideally human liver isozyme source, of sufficient size and quality to obtain structural data by X-ray crystallography are presented. Methods of growing such crystals are also disclosed.
CN103446127A Application of Lycojaponicumin A in anti-Helicobacter pylori drug An in-vitro activity experiment shows that Lycojaponicumin A has high anti-Helicobacter pylori (Hp) activity. The Lycojaponicumin A can be applied to treatment of acute gastritis, chronic gastritis, stomach diseases, duodenal ulcer and the like and preparation of drugs for treating the acute gastritis, the chronic gastritis, the stomach diseases, the duodenal ulcer and the like. The application of the Lycojaponicumin A in preparation of an anti-Helicobacter pylori drug is disclosed for the first time. Due to the fact that the skeleton type is a novel skeleton type and the high anti-Helicobacter pylori inhibitory activity of the Lycojaponicumin A is previously unimagined, the possibility that other compounds give any revelation does not exist, and the Lycojaponicumin A has outstanding substantive characteristics and meanwhile has a remarkable improvement in prevention and treatment of Helicobacter pylori infection obviously.
CN101543481B Double-layer breviscapine sustained-release tablet and preparation method thereof The invention relates to a double-layer breviscapine sustained-release tablet. One layer is a rapid-release layer that comprises 15-20g of breviscapine and routine tablet additives which are 0.5-4 of the weight of the breviscapine and comprise one or more of the following components: starch, lactose, microcrystalline cellulose, mannitol, CMS-Na, talcum powder, magnesium stearate L-HPC, PVPP and croscarmellose sodium; and the other layer is a sustained-release layer which comprises 45-40g of the breviscapine and skeleton matrixes which are 0.5-4 of the weight of the breviscapine and can be hydroxypropylmethyl cellulose, ethyl cellulose, carbopol or stearic acid, and auxiliary skeleton materials such as acrylics and polyvinylpyrrolidone can be also added. The preparation method of the double-layer sustained-release tablet is as follows: the components are mixed according to the proportion and compressed on a double-layer tablet machine to form the double-layer sustained-release tablet.
US7291347 Solubility, permeability, and bioavailability; oral dosage A novel salt of O-desmethyl venlafaxine is provided, O-desmethylvenlafaxine succinate. Pharmaceutical compositions, dosage forms and methods of use are also provided.
CN101822654A Pentetate inhalant The invention discloses a pentetate inhalant. The pentetate is selected from calcium trisodium pentate and zinc trisodium pentate. The pentetate inhalant is selected from a pentetate aerosol, a pentetate spray and a pentetate powder (a dry powder inhalant). The pentetate inhalant is characterized in that the pentetate inhalant can inhale the pentetate through a lung to directly act on the lung inhaling radionuclides and directly complex with the radionuclides, and the pentetate inhalant is coughed out or absorbed in blood to be discharged by a kidney, thereby effectively clearing the radionuclides including lanthanum, cerium, praseodymium, neodymium, promethium, zirconium, niobium, and plutonium, which are deposited in the lung; and while the lung inhales the pentetate inhalant into the blood to complex with the radionuclides in the blood to be discharged by the kidney, thereby effectively clearing systemic contamination. The pentetate inhalant can be conveniently carried and used.
EP1133279B1 Method of producing vitamin powders The present invention relates in general to a method of producing a dry, free-flowing mixture of liquid tocopherols. The present invention also relates to a dry free-flowing vitamin powder.
CA2230492C Human growth hormone variants Human growth hormone variants are disclosed having enhanced affinity for the growth hormone receptor. Also disclosed are human growth hormone variants conjugated to one or more chemical groups, such as poly(ethylene glycol), which is believed to prolong the in vivo half-life of the variants.
US20100297665 Method for testing and screening p38 map kinase modifiers This invention provides methods for treating diseases associated with elevated p38 mitogen-activated protein kinase activity. Moreover, the invention provides methods for testing a candidate compound for a p38 mitogen-activated protein kinase modifying activity by calculating the level of relocalization of an SMN complex component from the cytoplasm to the nucleus of a cell. Additionally, the invention provides a kit and a system for calculating the same.
US20050059067 Using restriction fragment length polymorphism in tyrosine kinase varian t as diagnostic tool in detection of cell proliferative and inflammatory disorders This invention relates to polymorphisms in the human KDR gene and corresponding novel allelic polypeptides encoded thereby. In particular, the invention relates to two polymorphisms in the coding sequence of the KDR gene, each of which lead to an amino acid change in the sequence of expressed protein; three single nucleotide polymorphisms (SNPs) in the promoter region; one SNP in the 5′ UTR and seven SNPs in intronic sequence. The invention also relates to methods and materials for analysing allelic variation in the KDR gene, and to the use of KDR polymorphism in treatment of KDR ligand (Vascular Endothelial Growth Factor VEGF)-mediated diseases such as cancer and various inflammatory diseases.
WO2011080651A3 Polymorphic forms of febuxostat The present invention provides crystalline forms of febuxostat, processes for their preparation, pharmaceutical compositions comprising them and their use for chronic management of hyperuricemia in patients with gout.
CA2293346C Device and method for treatment of dysmenorrhea Methods, devices, and compositions for treatment of dysmenorrhea comprise an intravaginal drug delivery system containing an appropriate pharmaceutical agent incorporated into a pharmaceutically acceptable carrier whereby the pharmaceutical agent is released into the vagina and absorbed through the vaginal mucosa to provide relief of dysmenorrhea. The drug delivery system can be a tampon device (42), vaginal ring, pessary, tablet, suppository, vaginal sponge, bioadhesive tablet, bioadhesive microparticle, cream lotion, foam, ointment, paste solution, or gel. The system delivers a higher concentration to the muscle of the uterus, the primary site for the dyskinetic muscle contraction, which is the pathophysiologic cause of dysmenorrhea.
CN101011489A Cordate houttuynia eye drops and its preparation method The invention relates to houttuynia cordata eye drops, which uses the houttuynia cordata extractive as active components, added with medical acceptable eye findings, wherein, the houttuynia cordata extractive contains 1.0mug-5.0mug/ml methyl nonyl ketone. The invention also provides relative preparation, while the drug quality is stable. And the methyl nonyl ketone is selected as the index component with controllable quality.
EP1889626A1 Hip kinase for fertility control The present invention relates to the use of a pharmaceutical composition which comprises as active component at least one HipK4 nucleic acid, a HipK4 polypeptide, modulators of HipK4, antibodies directed against HipK4, a HipK4 antisense, and a HipK4 RNAi, for the diagnosis and treatment of fertility impairments and for contraception. The invention further relates to the use of this pharmaceutical composition for manufacturing a medicament for the treatment of fertility impairments.
CN102786518A Palmatine hydrochloride crystal B substance, its preparation method, and its applications in medicines and healthcare products The invention discloses a new palmatine hydrochloride crystal B substance with the structure represented by formula (I), a preparation method of a palmatine hydrochloride crystal B sample, products prepared through treating the palmatine hydrochloride crystal B substance as an active component, and applications of the palmatine hydrochloride crystal B in the disease control and the healthcare, wherein the products comprise medicines and healthcare products.
CN101402641B Oxime derivatives containing thienopyridine, preparation method and application thereof The invention belongs to the anti-platelet aggregation drug technical field and provides oxime derivatives containing thieno pyridine with the structure as showed in general formula (I) and pharmaceutically acceptable salt thereof, wherein m=1, 2; n=0, 1; R<1>, R<2> and R<3> represent simultaneously or respectively hydrogen, C1-C6 linear chain or branched-chain alkyl, C3-C6 cycloalkyl, halogen, hydroxyl, carboxyl, amino, amido, cyano, nitryl, C1-C4 alkoxy, substituted phenyl and substituted heterocyclic radical; R<4> represents hydrogen, C1-C4 linear chain or branched-chain alkyl; the detailed definitions are described in the specification. The invention also relates to a preparation method of the compound, and meanwhile discloses a drug combination that uses the compound or the pharmaceutically acceptable salt as active ingredients and an application thereof as anti-platelet aggregation drugs.
CN102670690A Anti-psoriasis purely natural medicinal cream and preparation method thereof The invention discloses anti-psoriasis purely natural medicinal cream and a preparation method thereof. Main medicaments of the cream are active ingredients extracted from natural plants; and the cream has the characteristics of strong targeting property, low side effect, quick curative effect, low production cost and the like. The cream for treating psoriasis vulgaris or stubborn psoriasis has the advantages of quick response, high safety, relapse prevention and the like.
US8123707 Method and apparatus for connective tissue treatment The invention relates to methods and apparatus for therapeutically treating connective tissue or increasing vascularization in tissue using ultrasound. More particularly, the present invention relates to methods and apparatus which use ultrasound to stimulate growth or healing, or to treating pathologies, of connective tissue, or to increase vascularization in ischaemic or grafted tissue using ultrasound.
CN101717402A Pyrazolo N-substituted dehydronorcantharidin imide derivative and synthesis method and application thereof The invention discloses a pyrazolo N-substituted dehydronorcantharidin imide derivative and a synthesis method and application thereof, belonging to the technical field of cantharidin derivatives. In the invention, chloramine T is used for designing a simple and easy method of 1, 3-dipolar cycloaddition reaction, and the five-membered heterocyclic pyrazole ring is introduced into the methyl cantharidin substituted arylamine structure. The prepared novel pyrazole norcantharidin derivatives can be applied to the synthesis of antineoplastic drugs.
WO2005115993A1 Quinazoline derivative A compound represented by the formula (I): ring A (wherein R1 represents lower alkyl, etc.; R2 and R3 are the same or different and each represents hydrogen, etc.; R4 represents, e.g., a group represented by the formula (II): X1 represents NH, O, or S; Y represents N or C; Ar represents, e.g., a divalent group formed by removing two hydrogen atoms from aryl; and ring A represents a 5- or 6-membered heteroaryl, etc.) or a pharmaceutically acceptable salt of the compound. They have antagonistic activity against a histamine H3 receptor and inverse antagonistic activity against a histamine H3receptor and are useful in the prevention or treatment of metabolic system diseases, circulatory system diseases, or nervous system diseases.
US20110064717 Homing endonuclease genes and their targets The invention provides pharmaceutical composition having as an active ingredient either a homing endonuclease (HE) capable of cleaving a non-native target nucleotide sequence in a genome or a nucleotide sequence encoding for a HE capable of cleaving a target site in a non-native genome. The invention also provides uses for such HEs, and methods of treatment utilizing such HEs. The HE may be, for example, any one of the HEs PI-SceI, POLB HE, PRP8 HE, or Nostoc species PCC7120 HE.
CN102725293A A polymorph form of nevirapine and its preparation The invention relates to a metastable unsolvated crystalline form (Form- IV) of nevirapine, having at least one characteristic x-ray powder diffraction peak at approximately 7.1 DEG to 7.5 DEG two theta. The invention further relates to a preparation method of producing a particulate anhydrous unsolvated form of nevirapine.
EP0787206B1 USE OF NEURITE LOCALIZED mRNAs FOR MEDICAL DIAGNOSIS AND THERAPEUTICS A method of identifying neurite cDNA clones by determining and comparing mRNA expression in selected neurites is provided. cDNA clones identified by this method are also provided. In addition, methods of profiling mRNA expression and diagnosing and treating conditions associated with a pattern of mRNA expression by determining an mRNA expression profile are provided. The figure illustrates a differential display pattern obtained in neurites using the oligonucleotide OP-5 as the 3' primer.
US8680041 Genetic variations associated with tumors Nucleotide and amino acid variations associated with tumors are provided. Methods for detecting variations and for diagnosing and treating tumors are provided.
WO2013137284A1 Sulfur amino acid-containing composition Provided is a composition stably containing a sulfur amino acid, which is derived from an Allium plant, at a high concentration. A method for producing a sulfur amino acid-containing composition, said method comprising: a step for heating an Allium plant; a step for treating the heated Allium plant with a γ-glutamyl bond cleaving enzyme; and a step for subjecting the enzyme-treated product to ion exchange chromatography.
CN101103960B Dry mixed suspension containing racecadotril and preparation method thereof The invention provides a dry suspension agent containing racecadotril and the preparation method. The dry suspension agent provided in the invention contains a basic remedy ingredient with physiological available quantity and a carrier acceptable in pharmacy. The preparation method of the dry suspension agent containing racecadotril in the invention is characterized in that the basic remedy ingredient is firstly fixed evenly with a thinner and a suspending agent, then fixed with a wetting agent to produce granules in wet process, and finally fixed evenly with a corrective. The preparation method can hide the bitterness of medicine and guarantee the settling volume ratio of the dry suspension agent.
US20100286162 Human papilloma virus inhibitors and pharmaceutical compositions containing same HPV inhibitors of formula (I) in which G1 is —NHCO(CH2)n-, where n is an integer between 1 and 4, R3 is —CW(CH2)m—NR4R5 or —CW(CH2)mCH3 or —CN, where W is O, S or NH and m is an integer between 0 and 5, or R3 is one of the following groups: and A is an optionally substituted aryl group and B is an aryl group, preferably a phenyl which is substituted.
US20110112118 2,4-Diaminoquinazolines for Spinal Muscular Atrophy 2,4-Diaminoquinazolines of formulae I-IV and VI are useful for treating spinal muscular atrophy (SMA).
WO2014077787A1 Combinations including abeta2 agonist and glycopyrrolate Current invention related to pharmaceutical compositions containing glycopyrrolate and a β2-agonist which are used in treatment of asthma and chronic obstructive pulmonary disease.
CN103313701A Pharmaceutical compositions of pyridinium and quinolinium derivatives The present invention relates to pharmaceutical compositions comprising a compound of formula (I) and a cyclodextrin or a liposome, to the process of preparing said compositions and their use for antitumor, antiviral, antiparasitic and antifungal treatment.
US20100261656 Therapeutic Use of the Encoding Sequence of the Carboxy-Terminal Domain of the Heavy Chain of the Tetanus Toxin The present invention relates to the therapeutic use of the encoding sequence of the carboxy-terminal domain of the heavy chain of the tetanus toxin and of the polypeptide encoded by said sequence, preferably for the treatment of amyotrophic lateral sclerosis (ALS).
US20080306121 Bisheterocycle Tandem Compounds Useful as Antiviral Agents, the Uses Thereof and the Compositions Comprising Such Compounds The present invention provides small molecule compounds of bisheterocycle in tandem having the structural formula of P1-P2, and the use thereof as well as a composition containing the compounds, each of P1 and P2 is an unsaturated 5-member heterocyclic ring having one or two heteroatoms. This compound may effectively inhibit the replication of influenza virus, the DNA replication of hepatitis B virus (HBV), and the formation of HBsAg and HBeAg. These compounds can be used for the preparation of a medicament for viral diseases, and may overcome the limitations of the known nucleosides drugs, including cytotoxicity, the requirement of other drugs having different structures for against the drug-resistant virus variants induced by long-term therapy. The structure of the compounds according to the invention is relatively simple and easy to be prepared.
CN1594267A Diterpenoid monomer and its preparation method and application for preparing anti-cancer drugs Disclosed is an anti-cancer medicament ent-kauran-19-al-17-oic acid which is prepared by the steps of, (1) disintegrating the aired round lichee stems, extracting with ethanol, condensing into extract, (2) extracting with chloroform, column chromatography, purging and column chromatography again, and purging to obtain the end product.
CN103083263A Trovafloxacin ear drop pill for dogs and cats The invention discloses a trovafloxacin ear drop pill for dogs and cats. The pill is especially suitable for exudative and suppurative otitis media, and has the characteristics of fast drug release, no greasy feeling, easy cleaning, good stability, and convenient application, etc. The drop pill provided in the invention comprises, by mass: 12%-16% of trovafloxacin, 45%-70% of polyethylene glycol 6000, 15%-25% of polyethylene glycol 400, and 15%-25% of Tween 80. The trovafloxacin ear drop pill provided in the invention has the advantages of simple preparation process, high bioavailability, and good curative effect.
CN101590079A Calcium supplement health care product and production method thereof The invention discloses a calcium supplement health care product and a production method thereof, and relates to the technical field of biological health care food production process. The production method comprises the following steps: mixing and heating yolk protein, yolk oil and yolk lecithin to dissolution, adding egg white powder, yolk dry powder, egg membrance element powder and calcium carbonate powder, stirring evenly, and standing for 1 to 2 hours; adding 50-55 degree absolute ethyl alcohol of which the volume is twice of that of the mixture, sealing and standing for 5 to 8 hours; and removing ethanol by centrifugation, crushing a solid phase, and drying at vacuum to obtain the calcium supplement health care product. The calcium supplement health care product has simple process, environmental protection in the production process, good quality, no loss of nutrient components in the production process, and the retention period of 18 months, has no side effect after long-time use, is easy to be absorbed by human bodies, and is particularly suitable for osteoporosis, osteoarticular injury, back pain, protrusion of lumbar vertebral disc and early symptoms of heart cerebrovascular disease.
CN101390836A Antifungal activity ophthalmopathy slow-release microparticle and use thereof The invention relates to an anti-fungal ophthalmopathy sustained-release milli-microcapsule and the application thereof. The anti-fungal ophthalmopathy sustained-release milli-microcapsule contains voriconazole and is characterized in that the sustained-release milli-microcapsule also contains biodegradable pharmaceutical high-molecular auxiliary material; the voriconazolen and the biodegradable pharmaceutical high-molecular auxiliary material construct homogenized milli-microcapsule with the diameter of 100nm-100um; wherein, the voriconazolen accounts for 2%-50% of the total weight of the milli-microcapsule; the molecular weight of biodegradable pharmaceutical high-molecular auxiliary material is 5000-1000000Dolton. The pharmaceutical high-molecular auxiliary material is selected from poly(lactide-co-glycolide), polylactic acid, polylactic acid-glycolic acid. The anti-fungal ophthalmopathy sustained-release milli-microcapsule is widely applicable to the direct medicine delivery treatment in vitreous cavity or the ocular fungal infection prevention. The anti-fungal ophthalmopathy sustained-release milli-microcapsule treats fungal endophthalmitis through direct sustained-release vitreous cavity medicine delivery, needs less medicine dosage and effectively maintains the medicine concentration for 3 months after once medicine delivery so that the medicine economy is greatly improved. The medicine dosage applied on the ocular part is less when common voriconazolen injection is delivered systematically; patients cannot endure if the direct vitreous cavity injection needs to be conducted 3 times a day.
EP2480228A1 Use of nicotinic acetylcholine receptor alpha 7 activators The invention concerns the use of a nicotinic acetylcholine receptor alpha 7 activators for the treatment, prevention or delay of progression of dyskinesia associated with dopamine agonist therapy in Parkinson's Disease.
US20050182119 Anticancer agents; e.g. 1-(4-aminosulfonylphenyl)-3-trifluoromethyl-5-(2,5-dimethylphenyl)-4,5-dihydropyrazole or 1-(4-aminosulfonylphenyl)-3-trifluoromethyl-5-[3,5-di(trifluoromethyl)phenyl]-4,5-dihydropyrazole; improved antitumor activity; colon cancer, bowel cancer, or prostate cancer The present invention relates to new substituted pyrazoline compounds, pharmaceutical compositions containing such compounds and the use of these compounds for the treatment of cancer, in particular for the treatment of brain cancer, bone cancer, lip cancer, mouth cancer, esophageal cancer, stomach cancer, liver cancer, bladder cancer, pancreas cancer, ovary cancer, cervical cancer, lung cancer, breast cancer, skin cancer, especially for the treatment of colon cancer and/or bowel cancer and/or prostate cancer.
CN1879602A An ocular gel preparation and preparation method thereof The invention relates to an eye gelatin preparation and process for preparation, which comprises pearl powder hydrolysate, boneol, minor element zinc, solubilizing agent, thickening agent, preservative agent, isotonic conditioning agent, pH regulator and sterilizing water for injection.
CN101972248B Famotidine composition for injection and preparation method thereof The invention relates to a famotidine composition for injection. The famotidine composition comprises famotidine and L-aspartic acid; and the preparation method of the composition comprises the following steps of: 1) preparing: placing the famotidine and the L-aspartic acid in a preparation tank in a weight proportion of 1 to 0.4, filling injection water, stirring to completely dissolve the materials and uniformly mixing; 2) performing aseptic filtration, sub-packaging and partially stoppering; and 3) freeze-drying under vacuum to prepare the composition. The composition has a simple formula,an advanced process, good appearance molding, uniform and stable quality, uniform and accurate content, no moisture and high stability.
EP1373231B1 3-heterocyclyl-propano-hydroxamic acid as pcp inhibitors Compounds of formula (I): (I), and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.
EP1940400A2 Use of enoxaparin for performing percutaneous coronary intervention Methods for performing percutaneous coronary intervention in a patient in need thereof comprising administering intravenously a bolus comprising an effective amount of enoxaparin sodium to the patient after sheath insertion and prior to the percutaneous coronary intervention are described. Also described are methods for preventing or treating thrombosis, such as thrombotic episodes, in a human percutaneous coronary intervention patient by treating that patient with enoxaparin.
CN103417503A Amoxicillin potassium clavulanate tablet and preparation technology thereof The invention discloses an amoxicillin potassium clavulanate tablet and a preparation technology of the amoxicillin potassium clavulanate tablet. In the tablet, the weight ratio of amoxicillin and potassium clavulanate is 4-8:1. The tablet is formed by even mixing of amoxicillin granules, potassium clavulanate granules and auxiliary materials in a direct tablet compressing mode, wherein the auxiliary materials are acceptable in pharmacy. After the amoxicillin is screened, absolute ethyl alcohol granules are added, and the amoxicillin granules are obtained after drying. The potassium clavulanate is screened and then suspended in methylene chloride solution of hydroxypropyl methyl cellulose, drying is performed, methylene chloride is removed and therefore the potassium clavulanate is obtained. After the potassium clavulanate is wrapped, stability of the medicine is improved, and after granulation is performed on the amoxicillin, direct tablet compressing is facilitated.
CN102335279A Chewable tablet for removing garlic smell in oral cavity The invention relates to a chewable tablet for removing a garlic smell in an oral cavity. The chewable tablet comprises 20-100% of tomato powder, and when the content of the tomato powder is smaller than 100%, fillers and/or flavoring agents can make up for the balance. The fillers can be starch, milk powder, gum base for chewing gum, bifidus factors, lactobacillus, bifidobacterium, vitamins and/or aloe powder. The flavoring agents can be glycyrrhizin, glucose, fructose, cane sugar, essences and/or table salt. The chewable table provided by the invention comprises the following components in percentage by weight in preferential collocation: 70-98% of the tomato powder, 1-29% of the bifidus factors, and 0.1-2% of the glycyrrhizin. After a person eats garlic, the chewable tablet is molten or chewed in the mouth so as to effectively remove the garlic smell in the oral cavity; and by adding the bifidus factors and the glycyrrhizin and other fillers and flavoring agents into a product of the chewable tablet, the chewable table not only has the function of removing the garlic smell in the oral cavity but also has the effects of promoting appetite and supplementing natural vitamins and the bifidus factors.
US7422886 Human Phosphoinositide I3 Kinase p110 Delta which interacts with p85, has a broad phosphinositide specificity and is sensitive to the same kinase inhibitors as PI3 Kinase p110A; selectively expressed in leucocytes; enhanced expression in most melanomas The invention relates to a novel lipid kinase which is part of the PI3 Kinase family. PI3 Kinases catalyze the addition of phosphate to inositol generating inositol mono, di and triphosphate. Inositol phosphates have been implicated in regulating intracellular signaling cascades resulting in alternations in gene expression which, amongst other effects, can result in cytoskeletal remodeling and modulation of cellular motility. More particularly the invention relates to a novel human PI3 Kinase, p110Δ which interacts with p85, has a broad phosphinositide specificity and is sensitive to the same kinase inhibitors as PI3 Kinase p110A. However, in contrast to previously identified PI3 Kinases which show a ubiquitous pattern of expression, p110Δ is selectively expressed in leucocytes. Importantly, p110Δ shows enhanced expression in most melanomas tested and therefore may play a crucial role in regulating the metastatic property exhibited by melanomas. The identification of agents that enhance or reduce p110Δ activity may therefore prevent cancer metastatis.
US20110045032 Composition, formulations & kit for treatment of respiratory and lung disease with dehydroepiandrosterone(s) steroid & an anti-muscarinic agent(s) A pharmaceutical or veterinary composition comprises a non-corticosteroids, and/or salts thereof, and an anti-muscarinic (anti-cholinergic) agent, and/or pharmaceutically or veterinarily acceptable salts thereof. The composition is provided in various formulations and in the form of a kit. The products of this patent are useful in the prophylaxis and treatment of various respiratory, lung and malignant diseases.
WO2007071045A1 Catecholamine regulated protein A novel family of mammalian catecholamine proteins is identified. These proteins are useful in methods of diagnosing neurological diseases, including schizophrenia and bipolar disease, as well as cardiovascular disease. This family of CRP40 proteins are also useful to treat neurological diseases.
CA2587566A1 Heterocyclylbiphenyl derivates as protein tyrosine phosphatase inhibitors Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
US20080095718 Atomizing a phosphodiesterase inhibitor, receptor agonists of dopamine, melaocortin, or growth hormone-releasing peptide, or an alpha-adrenoceptor antagonist; with a hand-held delivery device; increased bioavailability; side effect reduction Methods are provided for increasing libido and/or treating erectile dysfunction in a man. The methods include the administration of a formulation testosterone alone, another fast-acting drug to treat erectile dysfunction or a combination of the testosterone and the other drug where at least one is delivered by aersolization. The formulation is preferably aerosolized and inhaled into a patient's lungs where particles of testosterone and/or the fast-acting erectile dysfunction drug deposits on lung tissue and then enter the patient's circulatory system.
US20110091548 Use of a matrix for orally administering sustained release magnesium, and composition containing said matrix A tablet for oral administration comprises a matrix of progressive and continuous released magnesium. For the administration of 90 to 110 parts by weight of magnesium, the matrix comprises 180 to 190 parts by weight of hydroxypropylmethylcellulose, 19.8 to 22.2 parts by weight of glyceryl behenate, 10 to 12 parts by weight of lactose and 10 to 12 parts by weight of colloidal silica. A non-enteric protective coating that slows down the gastric dissolution of the magnesium may comprise 15 to 75 parts by weight of shellac, cellulose ether or a mixture thereof. The tablet may be administered to patients in need thereof.
CN103705936A Preparation method of fish collagen double sustained-release film The invention relates to a fish collagen double sustained-release film and a preparation method thereof. An anti-tumor drug is encapsulated by biotin-coupled cholesteric glycol chitosan self-aggregated nanoparticles, and then drug-loaded nanoparticles are compounded with waste fish skin collagen and chitosan, so as to prepare the fish collagen double sustained-release film in manners of freezing and drying. The film has the advantages that local slow release is carried out, toxic and side effects of the whole body are reduced, and the like.
CN101647842B Fructus Podophylli extract and application thereof The invention relates to a Fructus Podophylli extract and an application of the extract and active ingredients in the extract to the preparation of a medicament for treating breast cancer. The Fructus Podophylli extract contains podophyllotoxin, deoxypodophyllotoxin, 4'-demethyldeoxypodophyllotoxin, 8-isopentenylkaempferol and a new compound of 8,2'-diprenylquercetin3-methyl ether. The experimentof the inhibited effect of the Fructus Podophylli extract and compounds on human breast cancer cells shows that the Fructus Podophylli extract and the compounds have the effect of inhibiting breast cancer cells. Besides, the compatibility use of podophyllotoxin lignanoids and isopentenyl flavone ingredients has the cooperative function and can remarkably improve the effect of inhibiting the breast cancer cells.
WO2010086349A1 Anti-inflammatory macrolide The compound 3'-N-demethyl-4"-O-(2-diethylaminoethanoyl)-6-O-methyl-9a-aza-9a- homoerythromycin A, having the Formula (I): or a salt thereof, compositions comprising the compound, its use in the treatment of neutrophil dominated inflammatory diseases, and methods for its preparation.
CN103494801A Action mechanism of silybin for preventing liver apoptosis through FXR (Farnesoid X Receptor) path The invention relates to the field of natural medicines, and in particular relates to an action mechanism of silybin for preventing liver apoptosis through an FXR (Farnesoid X Receptor) path. According to the invention, the silybin prevents apoptosis of HepG2 cells caused by ActD/TNF alpha through an FXR dependent path. Within human hepatoma cell line HepG2 cells, silybin can induce up-regulation of mRNA level and protein level of FXR in a dose-dependent manner, and can reverse down-regulation of FXR expression in a HepG2 cell apoptosis model caused by ActD/TNFalpha remarkably; the silybin has remarkable protective effect on the HepG2 cell apoptosis caused by the ActD/TNFalpha, but the anti-apoptosis function of the silybin is lost after the FXR SiRNA is used for silencing endogenous FXR genes.
CN102988366A Use and nasal administration medicine of hydroxycamptothecine The invention provides use of hydroxycamptothecine in preparation of nasal administration medicine for treating intracranial tumor. The invention further provides the nasal administration medicine of the hydroxycamptothecine. The nasal administration medicine of the hydroxycamptothecine can avoid a blood brain barrier, achieves larger enrichment in a brain tissue, and effectively solves the problem that the existing hydroxycamptothecine can not reach effective concentration in a cranium. Simultaneously, the nasal administration medicine of the hydroxycamptothecine adopts a specific auxiliary material type, use amount and a pH condition, avoids adverse reaction of the hydroxycamptothecine, preservative and the like on human bodies, is free of skin toxicity, increases compliance of patients, and provides a new route of administration for the hydroxycamptothecine for treating the intracranial tumor.
EP1392323B1 Use of a vitamin d3 analogue for the treatment of autoimmune diabetes The present invention is concerned with the use of 1,25-dihydroxy-16,23Z-diene-26,27-hexafluoro-19-nor vitamin D3 for the manufacture of a medicament for the prevention and/or treatment of autoimmune diabetes as well as for the manufacture of a medicament for preventing and/or treating allograft rejection. it is further concerned with a method for preventing and/or treating such diseases by administering 1,25-dihydroxy-16,23Z-diene-26,27-hexafluoro-19-nor vitamin D3 in an amount effective to prevent and/or to treat such diseases alone or in combination with other immunosuppressive agents.
CA2321265C Antibacterial compositions with synergistic effect, drugs and remedies for digestive diseases containing the same, process for the production thereof and preparations associated therewith Antibacterial compositions comprising (1) a rifamycin derivative represented by the formula (I) or its physiologically acceptable salt, and (2) a proton pump inhibitor (a) or a bismuth preparation (b) wherein the components (1) and (2) are used in such amounts as producing a synergistic effect against Helicobacter pylori, drugs and remedies for digestive organ diseases which contain the antibacterial compositions, process for producing them, and pharmaceutical preparations related to the antibacterial compositions. The compositions can be administered to patients with digestive diseases caused by infection of Helicobacter pylori in a smaller dose and at a lower administration frequency as compared with conventional remedies.
EP1494682A2 Polyphosphonate derivatives for toothpaste compositions The invention relates to a medicament containing the polyphosphonate compound of general formula (I) as an active ingredient.
EP1556029A2 Thiomolybdate analogues and uses thereof The current invention provides novel thiomolybdate derivatives, methods of making novel thiomolybdate derivatives, pharmaceutical compositions of novel thiomolybdate derivatives, methods of using novel thiomolybdate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-κB dysregulation and methods of using pharmaceutical compositions of thiomolybdate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-κB dysregulation.
US20100062968 Novel strategies for delivery of active agents using micelles and particles The present invention provides biodegradable particles (e.g., three-dimensional particles) and micelles which can be used to encapsulate active agents for delivering to a subject. The present invention further provides methods for producing and delivering such particles and micelles. Additionally, the invention provides vaccination strategies that encompass the use of the novel particles and micelles.
WO2004018999A3 Compositions, kits, and methods for identification, assessment, prevention, and therapy of cervical cancer The invention relates to nucleic acid molecules and proteins associated with cervical cancer including pre-malignant conditions such as dysplasia. Compositions, kits, and methods for detecting, characterizing, preventing, and treating human cervical cancers are also provided.
WO2012003784A1 Pyrazine derivatives,process for manufacture and use thereof Pyrazine derivatives of formula (I) and pharmaceutically acceptable salts thereof are disclosed, wherein the designation of R1, R2, R3 and R4 are provided herein. Syntheses for preparation of such compounds are disclosed. Methods of use of these compounds and pharmaceutical compositions containing them for treatment and/or prevention of diseases and for manufacture of medicaments are disclosed. These compounds and pharmaceutical compositions have antioxidative and thrombolytic effects, and thus can be used for the treatment and/or prevention of cerebral stroke caused by ischemia, and used for manufacture of medicaments for the treatment and/or prevention of nervous system diseases caused by excessive amount of radicals and/or thrombosis, infectious diseases, metabolic system diseases, cardiovascular and cerebrovascular diseases, and age-related degenerative diseases.
EP2493293A1 Methods for maintaining eye health and ameliorating opthalmic maladies in canines The invention provides novel methods for maintaining eye health and ameliorating ophthalmic maladies in canines by administering to the canines an ophthalmic malady ameliorating amount of one or more carotenes. Generally, the carotenes are administered to the canines in amounts of from about 0.1 to about 5000 mg or in amounts of from about 0.1 to about 500 mg per day to ameliorate maladies such as impaired vision, cataracts, cloudy eye, retinal degeneration, eye injury caused by radiation, reducing or preventing a decline of social interaction, promoting overall health and wellness, improving the quality of life, and extending the prime for canines.
CN1759842A Clathrate of Breviscapine, medication composition of containng clathrate of Breviscapine, and preparation method An inclusion compound of breviscapine, the composite medicine containing it and their preparing processes are disclosed. Said inclusion compound is prepared from breviscapine and beta-cyclodextrin in molecular ratio of 1: (0.5-3) through respectively preparing their solutions, mixing at 60-80 deg.C, including reaction, depositing, washing and drying. Said composite medicine is prepared from said inclusion compound and the pharmacologically acceptable carrier through mixing, sieving and conventional shaping.
US20090036495 Combinations Comprising Alpha-2-Delta Ligands and Ep4 Receptor Antagonists The instant invention relates to a combination of an EP4-receptor antagonist and an alpha-2-delta ligand, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly inflammatory, neuropathic, visceral and nociceptive pain.
US20130012533 Controlled release oxycodone compositions A method for preparing a solid oral dosage form comprising up to about 160 mg of oxycodone or a salt thereof to control pain in substantially all patients is disclosed. The method comprises wet granulating at least one hydrophilic or hydrophobic polymer, preferably a hydroxyalkyl cellulose or an alkyl cellulose, with oxycodone or a salt thereof to form a controlled-release matrix. Repeated “q12h” (i.e., every 12 hour) administration of the dosage form through steady-state conditions results in a mean maximum plasma concentration of oxycodone up to about 240 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration up to about 120 ng/ml from about 10 to about 14 hours after administration.
WO2007060112A1 Salicylic acid derivatives The present invention refers to O-acyl salicylic acid derivatives (I) bearing a NO donor moiety, a process for their preparation and pharmaceutical compositions containing them. (I) wherein : D is ONO2 or (A).
US20110177138 Alcohol-resistant sustained-release oral pharmaceutical form based on microgranules Oral pharmaceutical form containing microgranules for the sustained release of at least one active principle, including a neutral carrier that is insoluble in water or in an alcohol solution, or a neutral carrier rendered insoluble in water or an alcohol solution, comprising at least one first mounting layer containing at least one active principle and optionally a pharmaceutically acceptable binding agent, wherein the whole comprises at least one coating based on at least one hydrophobic polymer.
WO2008148710A2 Aryloxazole, aryloxadiazole and benzimidazole derivatives as modulators of somatostatins receptor activity This invention relates to compounds of the formula (I) wherein X is O or NR8, Y is CR7 or N, and R1 to R8 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
CN102018674A Diclofenac sodium hydrogel microballoon with pH sensitivity, preparation method and application thereof The invention relates to a diclofenac sodium hydrogel microballoon with pH sensitivity, a preparation method and application thereof. In the invention, chitosan and sodium alginate are used as drug carriers to prepare a diclofenac sodium hydrogel microballoon slow release preparation; the mass ratio of a used diclofenac sodium drug to the chitosan to the sodium alginate is (1-3):(5-8):(5-8); and the chitosan is N-succinyl-chitosan. The microballoon preparation can durably develop the drug effect to ensure that diclofenac sodium can be regularly and quantitatively released for a long time; after the microballoon preparation is taken, the blood concentration is stable, the fluctuation is small, and the duration time is long; the microballoon preparation has pH sensitivity, thereby irritations and toxic hazards to the stomach mucous membrane, which are caused by directly and orally taking diclofenac sodium tablets, are reduced; and the microballoon preparation has good effects of cooling down and easing pains and is suitable for various rheumatisms, rheumatoid arthritis, lupus erythematosus, ankylosing spondylitis, various pains caused after operations, fevers caused by various reasons, and the like.
CN102319229A Preparation method of diclofenac sodium transdermal patch The invention relates to a preparation method of a diclofenac sodium transdermal patch. The method comprises the following steps: 1) weighing 2 to 10 weight parts of azone, 2 to 10 weight parts of propylene glycol and 5 to 15 weight parts of absolute ethanol, uniformly stirring, and adding the mixture into 50 weight parts of diclofenac sodium for uniformly stirring; 2) weighing 200 to 300 weight parts of pressure-sensitive adhesive; 3) adding the mixture in step 1) into the substance in the step 2), stirring for 10 to 30 minutes, and homogenizing by using a homogenizer; and 4) uniformly coating a medicinal base layer to a release film, controlling the thickness to be between 40 and 60 mu m, and coating a medical elastic cloth. The preparation method has simple preparation process, and no bubbles are generated after the medicaments are applied.
WO2008138753A1 Hetarylanilines as modulators for amyloid beta The invention relates to compounds of formula (I) : wherein hetaryl I is formula (II); hetaryl II is formula (III); or to pharmaceutically active acid addition salts. It has been found that the present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease.
CN102872120A Application of Houttuynoid B in medicament for preventing or treating pancreatic fibrosis The invention discloses application of Houttuynoid B in preparing a medicament for preventing or treating pancreatic fibrosis. The use of Houttuynoid B in preparing the anti-pancreatic fibrosis medicament involved in the invention is disclosed for the first time; as the framework type of Houttuynoid B is a brand new framework type and Houttuynoid B has an unexpectedly high inhibition activity for the pancreatic fibrosis without possibility of giving any implication by other compounds, Houttuynoid B has outstanding substantive features; and simultaneously, the application of Houttuynoid B for preventing the pancreatic fibrosis apparently has obvious progress.
CN1846703A Vagina administration mifepristone prepn and its composition and prepn process The vagina administrated mifepristone preparation for birth control and health reproduction consists of mifepristone or nanometer mifepristone liposome particle as main component, excipient, osmosis promoter, pH regulator, preservative, surfactant, solvent, water and other pharmaceutically acceptable components, and may be prepared into gel, film or other preparation forms. The vagina administrated mifepristone preparation is absorbed through vagina mucous membrane into blood circulation, and has high bioavailability, lowered dosage, less toxic side effect and less stimulation.
WO2014031815A1 Pyrazolopyrimidine compounds Compounds of formula (I) and salts thereof : wherein R1 is n-C1-6alkyl or C1-2alkoxyC1-2alkyl-, R2 is halo, OH or C1-3alkyl, m is an integer having a value of 4, 5, 6 or 7, n is an integer having a value of 0, 1, 2 or 3, and p is an integer having a value of 0, 1 or 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
CN102068703A Doxorubicin multi-targeting drug delivery system and preparation method and application thereof The invention relates to a tumor cell multi-targeting drug delivery system, a preparation method of the drug delivery system and the application of the drug delivery system to anti-tumor drugs. The system is prepared by mixing a polyethylene glycol-hyaluronic acid-doxorubicin (PEG-HA-DOX) component and a Fe3O4 magnetic fluid component in the weight ratio of 1:(1-5), wherein the PEG-HA-DOX component comprises the following components in part by weight: 20 to 100 parts of doxorubicin, 500 to 1,500 parts of PEG, 100 to 500 parts of HA, 10 to 50 parts of dicyclohexylcarbodiimide (DCC), 1 to 10 parts of dimethylamino pyridine (DMAP), 100 to 500 parts of succinic anhydride, 10 to 50 parts of ethylidene dichloride (EDC) and 20 to 100 parts of sodium hydrogen sulfite. The system has the advantages of 1) drug releasing intelligence, 2) multi-targeting and good drug resistance reversion effect, 3) controlled drug releasing, 4) high blood circulation stability, 5) high invisibility and 6) wide applicability.
WO2013084153A1 Pharmaceutical composition comprising a trpa1 antagonist and an anticholinergic agent The present invention relates to a pharmaceutical composition comprising a transient receptor potential ankyrin-1 receptor ("TRPA1") antagonist and an anticholinergic agent. Particularly, the present invention provides a pharmaceutical composition comprising a TRPA1 antagonist having IC50 for inhibiting human TRPA1 receptor activity of less than 1 micromolar and an anticholinergic agent; a process for preparing such composition; and its use in treating a respiratory disorder in a subject.
WO2012161358A1 Pharmaceutical composition for preventing or treating attention deficit hyperactivity disorder (adhd), containing ginkgo leaf extract with enhanced terpenlactone The present invention relates to a pharmaceutical composition for preventing or treating attention deficit hyperactivity disorder (ADHD), and more specifically, to a pharmaceutical composition for preventing or treating ADHD, containing a ginkgo leaf extract with enhanced terpenlactone. In addition, the pharmaceutical composition of the present invention can further comprise a ginseng extract with enhanced prosapogenin such as ginsenoside Rg3 and the like. The pharmaceutical composition of the present invention is enhanced in terpenlactone compared with a conventional ginseng leaf extract or ginseng extract, and is thus effective for improving brain function disorders and enhancing cognition, and in particular, can remarkably prevent or treat ADHD.
US7208512 Benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma The present invention provides benzodifuran imidazoline derivatives and benzofuran imidazoline derivatives for lowering intraocular pressure and providing ocular neuroprotection.
CN101984968A Preparation method of pharmaceutical preparation of antitumor agent temozolomide The invention relates to a preparation method of the pharmaceutical preparation of antitumor agent temozolomide. The aim of the invention is to make up for the defects of the prior art and provide a safe, effective and stable new preparation for a large number of patients and medical workers, wherein the new preparation is convenient to take and can increase the bioavailability and blood concentration of the medicine, shorten the peak time and increase the antitumor fuction. The preparation method of the freeze-dried powder injection of the antitumor agent temozolomide is that temozolomide is used as the raw material, certain kinds of accessories in a defined ratio are added in the raw material, and the freeze drying technology of the pharmaceutics is utilized to prepare the freeze-dried powder injection.
CN1568957A Reforming effect of arginine to recessive harm of skin tissue of diabetic The invention discloses the novel use of arginine in preparing therapeutic medicine compositions for treating skin recessive damage caused by diabetes, wherein the medicament can make the diabetes patient's skin recover to near the normal thickness.
US7294620 Lipid analogs for inhibiting HIV-1 activity The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the activity of the viral infection.
CN103705943A Preparation method and application of reduction-response-type pegylation (PEG) nanomedicine composition The invention relates to a preparation method and application of a reduction-response-type pegylation (PEG) nanomedicine composition. The nanomedicine composition is characterized by being prepared by coupling the PEG with a medicine via disulfide bonds which are sensitive in reduction. Thus, the water solubility of the medicine is improved; the in-vivo behavior of the medicine is also improved. Meanwhile, the full release and the activity of the medicine are ensured by utilizing the characteristic that the disulfide bonds in the PEG medicine, which are sensitive in reduction, can be specifically degraded in a tumor site. Thus, a good tumor treatment scheme is provided.
WO2014094178A1 Radiosensitizer compounds for use in combination with radiation Disclosed herein are radiosensitizer compounds useful in combination with radiation therapy, e.g., a synergistic combination therapy for the treatment of cancer and other disorders. The radiosensitizer compounds have the general formula I: wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the radiosensitizer compounds are also disclosed.
WO2007010999A1 Animal in which lipid metabolism and sugar metabolism are modified by krap gene mutation, modification method and modifying agent It is intended to provide a novel agent which can contribute to prevention and/or treatment of obesity and/or diabetes, a transgenic animal which can be used for the purpose of elucidating pathologic conditions of such as obesity and/or diabetes or the like, a nucleic acid molecule which can be used for the production thereof and the like. One aspect of the invention is a transgenic nonhuman animal in which the expression of KRAP gene is reduced or lost.
WO2010129276A2 PYRO-GLUTAMATE Aβ TARGETING AGENTS A method of inhibiting amyloid beta aggregation in a mammal includes administering an amount of a pyro-Glu-(3-40/42)-Aβ targeting agent and/or fragment thereof that specifically binds to an epitope of the N terminus end of a pyro-Glu-(3 -40/42)- Aβ effective to inhibit amyloid beta aggregation in the subject.
US7144886 Dipeptidyl peptidase IV (DP-IV) inhibitors as anti-diabetic agents The present invention relates to a series of prodrugs of inhibitors of DP-IV with improved properties. The compounds can be used for the treatment of a number of human diseases, including impaired glucose tolerance and type II diabetes. The compounds of the invention are described by general formula (1); wherein R1 is H or CN; R2 is selected from CH2R5, CH2CH2R5 and C(R3)(R4)—X2—(CH2)aR5; R3 and R4 are each independently selected from H and Me; R5 is selected from CON(R6)(R7), N(R8)C(═O)R9, N(R8)C(═S)R9, N(R8)SO2R10 and N(R8)R10; R6 and R7 are each independently R11(CH2)b or together they are —(CH2)2—Z—(CH2)2— or CH2—o—C6H4—Z—CH2—; R8 is H or Me; R9 is selected from R11(CH2)b, R11(CH2)bO and N(R6)(R7); R10 is R11(CH2)b; R11 is selected from H, alkyl, optionally substituted aryl, optionally substituted aroyl, optionally substituted arylsulphonyl and optionally substituted heteroaryl; R12 is selected from H2NCH(R13)CO, H2NCH(R14)CONHCH(R15)CO, C(R16)═C(R17)COR18 and R19OCO; R13, R14 and R15 are selected from the side chains of the proteinaceous amino acids; R16 is selected from H, lower alkyl (C1–C6) and phenyl; R17 is selected from H and lower alkyl (C1–C6); R18 is selected from H, lower alkyl (C1–C6), OH, O-(lower alkyl (C1–C6)) and phenyl; R19 is selected from lower alkyl (C1–C6), optionally substituted phenyl and R20C(═O)OC(R21)(R22); R20, R21 and R22 are each independently selected from H and lower alkyl (C1–C6); Z is selected from a covalent bond, —(CH2)c—, —O—, —SOd— and —N(R10)—; X1 is S or CH2; X2 is O, S or CH2; a is 1, 2 or 3; b is 0–3; c is 1 or 2; and d is 0, 1 or 2.
WO2009134754A1 Benzoimidazole glycinamides as prolyl hydroxylase inhibitors The present invention is directed to benzoimidazole compounds of the formula: I and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
US20080254042 Using prolactin-releasing peptide (PrRP) to identify modulators for prevention and treatment of nervous system, heart, hepatic and anxiety disorders The present invention relates to provision of a method of screening a medicament using a disease-associated gene product, an antibody to the disease-associated gene product, and an antisense DNA which suppresses expression of the disease-associated gene product. Specifically, the present invention provides a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, its partial peptide, or a salt thereof.
US20080125418 Benzimidazole derivatives and their use as kdr kinase protein inhibitors The invention discloses and claims benzimidazole compounds of formula (I): wherein X is C—R2; Y is C—R2 or C—R3; W and Z are each C—R3; R1 is an optionally substituted aryl, heteroaryl or a saturated 5- or 6-membered monocyclic heterocyclic radical or a bicyclic heterocyclic radical; and A5 is H or alkyl; or a stereoisomer, a racemate, an enantiomer or a diastereoisomer of said compound of formula (I) or a pharmaceutically acceptable salt thereof; the use of compounds of formula (I) for the treatment of a disorder of proliferation of blood vessels, uncontrolled angiogenesis, a fibrotic disorder, a disorder of proliferation of mesangial cells, a metabolic disorder, allergy, asthma, thrombosis, a disease of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration, solid tumors and cancers, pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents and pharmaceutical compositions comprising a compound of formula (I) and one or more. antimitotic agents.
US20120071452 Combinations comprising antimuscarinic agents and corticosteriods Combinations comprising (a) a corticosteroid and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary disease.
US20120232118 Selective ligands for the dopamine 3 (d3) receptor and methods of using the same Potent and selective ligands for the dopamine 3 (D3) receptor are disclosed. The D3 receptor ligands have a structural formula: wherein R1 is C1-6 alkyl or C3-6cycloalkyl; or wherein R2 is substituted with one or two halogen(s) or OC1-3alkyl.
EP2356090A2 Crystalline forms of fingolimod hcl The present invention relates to crystalline forms and hydrates of 2-Amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diol, and to the use thereof, in particular in the treatment or prevention of various autoimmune conditions.
CA2687931A1 Ccr2 receptor antagonists and uses thereof The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonarydiseases like asthma and COPD.
US20090298940 All Natural Antifungal And Antimicrobial Composition And Method Thereof In accordance with the present invention, there is provided a novel all natural antifungal composition and method. There is further provided a novel all natural antibiotic and antimicrobial composition and method. There is provided an antifungal and/or antimicrobial composition and method that may be used to treat conditions caused by gram negative bacteria, viruses and fungi, especially molds and mycocytes, with a composition comprising potassium sorbate, lecithin, cellulose, and wax. There is provided a composition and method for administration directly to dermal, oral, gastrointestinal and/or nasal tissues that are affected by molds and mycocytes.
CN102357139A Formula of special confined puerpera conditioning water and making process thereof The invention provides a formula of special confined puerpera conditioning water and a making process thereof, and relates to a making process for conditioning water. The making process comprises the following steps of: 1, pouring 9L of rice wine into a pot, not covering a cover to contribute to volatilizing alcohol, heating over intense fire until boiling, cooking over medium or slow fire, immediately covering the cover when fire reaches the edge of the pot, obtaining 3L after about 3 hours, and making brewed water; and 2, cleaning and airing raw materials in different stages, putting into earthen pots respectively, adding the brewed water, soaking for more than 3 hours, heating over intense fire until boiling, and decocting over slow fire for 1 hour, properly adding brown sugar or crystal sugar according to personal conditions, and uniformly stirring. The conditioning water can enrich blood and promote the circulation of qi, promote blood circulation, condition qi and blood of the whole body, avoid qi-blood deficiency and discomfort such as dizziness, weakness, dim eyesight, abnormal sweating due to general debility, and retention of lochia or less lochia after delivery, help a puerperal avoid cold, prevent a plurality of diseases such as postpartum joint pain and the like, activate blood circulation, stimulate meridians, warms spleen and stomach, and can promote milk secretion.
US7265095 Monoclonal antibody 3F1H10 neutralising VHSV (viral haemorrhagic septicaemia virus) The present invention relates to a non-infectious nucleic acid (RNA and DNA) construct constructed to express a recombinant antibody or antibody fragment in a host cell. The antibody molecule confers protection to the host against a pathogen, allergen or toxin. The host may be any animal including a human or a fish. More specifically, the antibody may be against viral haemorrhagic septicaemia virus.
CN101830877A Application of arnentobiflavone and derivatives thereof for preventing and treating radiation injury The invention relates to the novel application of arnentobiflavone and derivatives thereof for preventing and treating radiation injury. Proved by experiments, the arnentobiflavone is innoxious to V79 cells in a concentration range less than 20ug/ml, plays dose-dependent inhibiting effect on the activity loss of the V79 cells caused by 60Co gamma ray in the concentration range of 0.2-5ug/ml, can increase the survival rate of BALB/c mousse under 60Co gamma-ray 6Gy irradiation in a dose-dependent mode, therefore, the arnentobiflavone can be used for preventing and treating radiation injury.
CN101875655B Aminobenzoic acid derivative as well as preparation method and application thereof The invention relates to the field of blood coagulation. Specifically, the invention relates to a new aminobenzoic acid derivative with a structure in a general formula (1) in the specification, a preparation method thereof, medicament compositions containing same and application of the aminobenzoic acid derivative as a bioactive substance for preparing medicaments for preventing and/or treating diseases, wherein the definitions of all groups are described in the specification.
WO2013057619A1 Novel phenicol antibacterials The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical compositions containing these novel compounds, and methods for the preparation of these compounds.
CN103611152A Compound vitamin D electuary The invention discloses a compound vitamin D electuary. The electuary is mainly prepared from the following main raw materials: lotus root starch, casein phosphopeptides and vitamin D.
US20070281030 Non-Lamellar Compositions of Dope and P80 The present invention relates to particulate compositions comprising at least 50% of dioleoyl phosphatidyl ethanolamine (DOPE) and 1 to 50% of Polysorbate 80 (P80). All parts are by weight relative to the sum of the weights of a+b and the compositions comprise non-lamellar particles or form non-lamellar particles when contacted with an aqueous fluid. The compositions have advantageous stability and low toxicity and the invention also relates to pharmaceutical compositions thereof.
CN102138919A New application of sodium ferrous chlorophyll to promotion of erythropoiesis The invention discloses new application of sodium ferrous chlorophyll to the promotion of erythropoiesis, and belongs to the field of medicines. Sodium ferrous chlorophyll has the effect of erythropoietin, and can be prepared into medicaments for treating anemia such as 'anemia of chronic disease' or 'renal anemia' which are caused by hyposecretion in erythropoietin.
US20070276012 Process for Preparing Thiazolidinediones This invention provides a process for reducing an exocyclic double bond at the 5-position of a thiazolidinedione moiety of a thiazolidinedione precursor comprising the steps of: a) preparing a solution or suspension of the thiazolidinedione precursor in a non-ether solvent medium with a base, and b) combining the solution or suspension with a dithionite source. Preferred solvent media include aqueous N,N-dimethylformamide. Sodium dithionite is a preferred dithionite source.
US20110293599 Method for modulating muscle differentiation or regeneration Present invention relates to method for promoting or inhibiting muscle differentiation or regeneration using an enhancer or an inhibitor capable of modulating the binding of TAZ polypeptide with MyoD polypeptide; method for screening a substance capable of up- or down-regulating muscle differentiation or regeneration by use of interaction between TAZ polypeptide and MyoD polypeptide; an isolated peptide consisting of an amino acid sequence of SEQ ID NO. 2 which binds to and activates the MyoD polypeptide; a polynucleotide encoding the isolated peptide; and a pharmaceutical composition comprising the isolated peptide or the polynucleotide.
CN1676508A Anti-inflammatory and anti-thrombus compound and its medicinal composition This invention includes the new type of chemical compounds showed by constitutional formula 1, they are anti-inflammatory and anti-thrombus medicines. This invention also comprises certain chemical element and a method curing COX-1 and COX-2 adjusting disease, and meanwhile comprises the utilization of the chemical compounds illustrated by molecular formula 1. The above chemical compounds can be integrated with small dosage of aspirins, non-steroid anti-inflammatory medicine and selective COX-2 to cure chronic COX-1 COX-2 adjusting diseases or symptoms, and meanwhile reduce the dangers of heart and vein diseases caused by thrombus.
CN102603559A Phenylacetyl fluorobenzene salicylamide compound and application thereof The invention discloses a phenylacetyl fluorobenzene salicylamide compound shown as a formula (I), and discloses an application of the phenylacetyl fluorobenzene salicylamide compound to preparation of an antitumor medicament, in particular to an anti-endometrial carcinoma medicament. The invention has the beneficial effects that: (1) a phenylacetyl fluorobenzene salicylamide compound is provided; (2) a novel anti-endometrial carcinoma medicament with remarkable antitumor activity is provided, a research foundation is provided with screening of novel medicaments, and an important application prospect is achieved; and (3) the preparation flow is simple, and industrial production is facilitated.
WO2014139970A1 Processes and intermediates for preparing a medicament Disclosed is a process for the preparation of the following compounds: (I), (II) where R1, R1a and R2a have the definitions in the description, as well as a process to prepare other intermediates that may be useful to synthesise downstream products, especially compounds that are useful as medicaments, for instance Bruton's tyrosine kinase (Btk) inhibitors such as ibrutinib. Also disclosed are other processes, other intermediates and compounds per se.
US20120195911 Method of treatment of cancer patients This invention may be used in human and veterinary medicine in combination with traditional methods of treatment of oncological illnesses for the purpose of increasing their effectiveness. It is a method of treating patients with oncological diseases that is distinct in that an antiviral drug is used as an additional component of standard treatment before the beginning of and in parallel with standard treatment, in which Acyclovir, Valacyclovir, alpha interferon, a specific antiviral immunoglobulin or a combination of these substances are used as an antiviral drug, which may be used for inclusion in the standard surgical, radiological, or chemotherapeutic treatment plan for cancer patients. The proposed method allows us to significantly improve the results of the treatment of cancer patients, decrease the number of relapses, improve patients' quality of life, and significantly extend their lives. Because the proposed drugs are already approved for use, there are no technical difficulties facing their inclusion in cancer patients' treatment plans.
EP1224195B1 C-aryl glucoside sglt2 inhibitors SGLT2 inhibiting compounds are provided having formula (I) where R?1, R2, and R2a¿ are independently hydrogen, OH, OR5, lower alkyl, CF¿3?, OCHF2, OCF3, SR?5i¿ or halogen, or two of R?1, R2 and R2a¿ together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R?3 and R4¿ are independently hydrogen, OH, OR5a, OAryl, OCH¿2?Aryl, lower alkyl, cycloalkyl, CF3, -OCHF2, -OCF3, halogen, -CN, -CO2R?5b, -CO¿2H, -COR6b, -CH(OH)R6c, -CH(OR?5h)R6d, -CONR6R6a¿, -NHCOR5c, -NHSO¿2R?5d, -NHSO¿2?Aryl, Aryl, -SR?5e, -SOR5f, SO¿2R5g, SO2Aryl, or a five, six or seven membered heterocycle, or R?3 and R4¿ together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R?5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h, and R5I¿ are independently lower alkyl; R?6, R6a, R6b, R6c and R6d¿ are independently hydrogen, alkyl, aryl, alkylaryl or cycloalkyl, or R?6 and R6a¿ together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle; A is O, S, NH, or (CH¿2?)n where n is 0 - 3. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.
WO2007143422A3 Substituted pyridyl amide compounds as modulators of the histamine h3 receptor Pyridylamide compounds of Formula: (I); wherein R1 is -C1-4alkyl or saturated monocyclic cycloalkyl; m is 1 or 2; X is N or CH; Y is N or CR3; Ra is -H, -Z-Ar, -CH2NRbRc, -CN, -CO2C1-4alkyl, -CO2H, or -CONRbRc; where Rb and Rc are each independently -H or -C1-4alkyl; and R2 is -H or -Z-Ar; with the proviso that one of X and Y is N and one of Ra and R2 is -Z-Ar; where Z is O or S; and Ar is a phenyl or monocyclic heteroaryl group unsubstituted or substituted with one, two, or three R3 substituents; where each R3 substituent is independently selected from the group consisting of: halo, -C1-4alkyl, -OH1 -OC1-4alkyl, -SC1-4alkyl, -CN, -CONRdRe, and -NO2; where Rd and Re are each independently -H or -C1-4alkyl; are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated1 diseases.
US6881725 Administering to a subject a purine derivative to reduce traumatic pain, neuropathic pain, organ pain and pain associated with diseases The present invention is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and pain associated with diseases. The P2X receptor antagonists particularly useful for this invention are mononucleoside polyphosphate derivatives or dinucleoside polyphosphate derivatives of general Formula I. The compounds of the present method can be used alone to treat pain. The compounds of the present method can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the overall pain-reducing effect in a subject in need of such treatment.
CN103550774A Method for screening sound-sensitive agent in induction of mitochondrial pathway apoptosis The invention relates to a method for screening a sound-sensitive agent in induction of mitochondrial pathway apoptosis. The method comprises the following steps: (1) loading a medicine with sound sensitivity or a precursor of the medicine with sound sensitivity on cells, and giving ultrasound wave irradiation after the sound-sensitive agent is absorbed or transformed by the cells; (2) detecting the binding capacity of the sound-sensitive agent and the mitochondrial 18 kDa translocator protein (TSPO), and screening the sound-sensitive agent for inducting the mitochondrial pathway apoptosis. The invention provides a target spot for screening the sound-sensitive agent. The target spot is used for screening the sound-sensitive agent which can induce the mitochondrial pathway apoptosis. Moreover, an effective method is provided for screening sound-sensitive agent medicines, research and development of the sound-sensitive agent medicines are promoted, and theoretical research and clinical application of sonodynamic therapy are promoted.
EP1455774B1 Pharmaceutical composition for treating obesity A salt of N,N' sebacoyl bis-sarcosine [S(Sar)2] having the formula (CH2)8-[CO-N(CH3)-CH2-COOH]2 (SBS) with L-arginine or L-lysine is used for the treatment of obesity.
WO2007143897A1 A compound with special property, compositon comprising the compound and its preparation and uses A hydrate or dehydrate of calcium dibutyryladenosine cyclophosphate with special property, pharmaceutical composition comprising the compound, and its preparation and uses are provided. The molecular formula of the compound is C18H23N5O8P 1/2 Ca nH2O, wherein n=0~2.5. The compound is presented in the form of white-like or pale yellow powder, which is slight soluble in water and is almost unsolvable in alcohol. The compound with outstanding stability is proteinkinase activator, which is mainly used to treat cardiac cerabral vascular disease and to modulate the growth of mammal.
US20110144182 Treatment of surgical adhesions Connexin modulation for the treatment of surgical adhesions, and associated methods, compositions, and articles.
CA2166062C The use of non-ionic surfactants in stable topical retinoid compositions Compositions, comprising a retinoid in an aqueous vehicle, containing at least one crystallisation preventing and stabilising agent, are provided. Said agent is chosen from the group of non-ionic surfactants.
WO2013060668A1 New therapy for transthyretin-associated amyloidosis It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
CN102861090A Application of Houttuynoid C in medicine for treating bile duct cancer The invention discloses application of Houttuynoid C in preparation of a medicine for treating human bile duct cancer, belonging to the technical field of new application of medicine. The invention discovers that Houttuynoid C has the remarkable inhibitory effects on the growth of human bile duct cancer cell strain RBE through the evaluation of in vitro MTT antineoplastic activity. Therefore, Houttuynoid C can be used for preparing the anti-bile duct cancer medicine and has good development and application prospects. The application of Houttuynoid C in preparation of the medicine for treating bile duct cancer provided by the invention is disclosed firstly. The skeleton type belongs to new skeleton type, and the inhibitory activity of Houttuynoid C on human bile duct cancer cells is unexpectedly strong.
CN101670019A Complex preparation having radiation-resisting and eyesight-protecting functions The invention relates to a complex preparation having radiation-resisting and eyesight-protecting functions, which comprises the following components in percentage by weight: 65 to 98 percent of tea seed oil, 0.15 to 15.0 percent of coenzyme Q10, 0.05 to 10.0 percent of lutein, 0.10 to 10.0 percent of alpha-lipoic acid and 0.01 to 0.10 percent of vitamin A. The tea seed oil is grease obtained by picking and shelling mature seeds of tea trees, drying the shelled tee seeds by hot air at a temperature of between 100 and 110 DEG C until constant weight is achieved, smashing the tee seeds and extracting the tee seeds by using supercritical carbon dioxide. The five components are mixed organically to obtain an efficient radiation-resisting and eyesight-protecting product, so that defects of related products in the current market are solved skillfully. The complex preparation having the radiation-resisting and eyesight-protecting functions is particularly suitable for a wide range of people exposed under radiation environment and is a health-care food with the functions of preventing and repairing damages, protecting the eyesight and relieving asthenopia.
CN102219670A Linear chain polyketone compounds and application thereof The invention relates to the technical field of medicines, in particular to linear chain polyketone compounds separated from marine poriferans and application thereof in preparation of medicines for treating tumors, diabetes and obesity or inhibitors for protein tyrosine phosphatase-1B(PTP1B). The in vitro anti-tumor tests and the PTP1B inhibition tests show that the compound C17H32O4 has obvious inhibiting activity on human colon cancer cells HCT-116 and PTP1B, so that the compound can be used for preparing anti-tumor medicines or PTP1B inhibitors and medicines for treating diabetes, obesity and complications caused by diabetes and obesity. The invention provides novel lead compounds for developing new anti-tumor medicines or medicines for treating diabetes and obesity, and has great significance for the development and the utilization of Chinese marine medical biological resources.
EP2078712A1 Indole derivatives as selective androgen receptor modulators (sarms) The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
CN102600092A Method for preparing sinomenine hydrochloride tablets by non-organic solvents The invention relates to a method for preparing sinomenine hydrochloride tablets, in particular to method for preparing sinomenine hydrochloride tablets by non-organic solvents. In the method, conventional highly toxic benzene extraction and chloroform extraction (solvent extraction) processes are replaced by cation exchange resin or macroporous resin adsorption, the extraction yield is high, theoperation is easier, harms and pollution caused by large organic solvent dosage and large toxicity to the health of operators and the environment are overcome, the treating processes of organic solvents are reduced to be conductive to environment protection and environment-friendly production, and the investment in environmental protection facilities of plants is reduced. The sinomenine hydrochloride extracted and separated by the method disclosed by the invention is used as the raw material of pharmaceutical preparation, and has higher purity without solvent residue, and potential hazards tothe human body are reduced.
CN102579961A Quality control method for aristolochic acid A in swelling-reducing and pain-alleviating tincture The invention discloses a detection method for a swelling-reducing and pain-alleviating tincture, which is used for controlling the content of aristolochic acid A in the swelling-reducing and pain-alleviating tincture and ensuring that the content of aristolochic acid A in the swelling-reducing and pain-alleviating tincture meets the safety requirement of a product. Due to the adoption of the method provided by the invention, the detection problem of a small amount of aristolochic acid A is solved, and a high-sensitivity, accurate and reliable detection method for aristolochic acid A is established. On the aspect of operation, the method provided by the invention is accurate and reliable, and has high accuracy and very high practical value.
US20080249142 N-methyl-5-(5-isopropoxy-3-pyridinyl)-4-penten-2-amine p-hydroxybenzoate; compounds can activate nicotinic receptor and can modulate neurotransmitter secretion; neuroprotective agents; side effects reduction; pains; easy to remove impurities; heck coupling reaction; CNS disorders; inflammatory disorders Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine compound) or to another pharmaceutically acceptable salt form.
US20090035301 Methods for diagnosing and treating bladder cancer The present invention relates to the diagnosis and treatment of bladder cancer. More specifically, this invention uses the levels of macrophage migration inhibitory factor (MIF) produced by the bladder epithelia (urothelia) as a marker for bladder cancer. Moreover, the present invention also provides a method for attenuating bladder carcinoma by inhibiting of macrophage MIF.
US20110021641 Suspension formulation for carbon adsorbents The invention relates to an aqueous suspension formulation comprising a coarsely particulate carbon adsorbent which is suitable for binding and eliminating harmful substances from the gastrointestinal tract, and a water-soluble or water-dispersible structure-forming agent and a humectant.
US20120251499 Method for diagnosis/prognosis of cancers using an epigenetic marker consisting of a specific single cpg site in ttp promoter and treatment of cancers by regulating its epigenetic status The present invention relates to a method for the diagnosis and prognosis of cancers using an epigenetic marker consisting of a specific single CpG site in TTP (Tristetraprolin) promoter and treatment of cancers by regulating its epigenetic status. Particularly, the present invention relates to a method for the diagnosis and prognosis of liver cancer by measuring specific methylation of C, the 32nd residue of the nucleic acid sequence represented by SEQ. ID. NO. 41, and a method for treatment of cancer by regulating the same. The present invention can be effectively used for the diagnosis and/or treatment of liver cancer characterized by TTP down-regulation and methylation of C, the 32nd residue of the nucleic acid sequence represented by SEQ. ID. NO. 41. The present invention can be further applied for the diagnosis and treatment of other cancers or inflammatory diseases that are characterized by TTP down-regulation and methylation of C, the 32nd residue of the nucleic acid sequence represented by SEQ. ID. NO. 41.
WO2009072002A3 Bisphenols in cancer therapy The present invention generally relates to anticancer agents and methods of treating cancer. The anticancer agents described herein comprise a bisphenol core and generally act as topoisomerase II inhibitors, though their anticancer activity may be related to other mechanisms as well. The bisphenols discussed therein may also protect certain cells against detrimental effects of topoisomerase II poisons.
US7919489 e.g. 4-({[(4-Chloro-2-methylphenyl)amino]carbonyl}amino)-1-(cyclopropylmethyl)-1H-imidazole-2-carboxylic acid; antiviral agents, especially against cytomegaloviruses and other Herpes viridae; side effect reduction; antibiotic resistance The invention relates to heterocyclylamide-substituted imidazoles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the use as antiviral agents, especially against cytomegaloviruses.
WO2013072758A1 Pyrimidine diol amides as sodium channel blockers The present disclosure provides pyrimidine diol amides of Formula (I), and the pharmaceutically acceptable solvates and prodrugs thereof, wherein A1, X, A2, W1, W2, W3, R1, R2, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
WO2009020314A3 Stabilized alpha-lipoic acid particles, composition comprising the same and method for preparing the same The present invention provides stabilized α-lipoic acid particles, each of which includes a core consisting of α-lipoic acid particles having a volume average particle diameter of 3 to 30 μm and a first coating layer formed on the surface of the core wherein the first coating layer includes fine particles of an amino acid or an amino acid derivative or the like having a volume average particle diameter of 0.01 to 2.5 μm, a composition including the same, and a method for preparing the same.
WO2012107304A1 Histone deacetylase (hdac) inhibiting compounds and method of making same The invention relates to novel HDAC inhibitors and a method of making such HDAC inhibitors. The present invention provides novel HDAC inhibitors having a perfluorinated linker between the metal-binding group and the cap group.
US20090215714 Pyrimidines, such as cytidine, in treatments for patients with biopolar disorder The invention is based on the discovery that specific dosages of pyrimidine compositions, such as cytidine compositions, can be used to treat patients diagnosed with bipolar disorder.
EP1928425A1 Pharmaceutical formulation containing an hmg-coa reductase inhibitor and method for the preparation thereof The present invention relates to improved pharmaceutical formulation for oral administration comprising a therapeutically effective quantity of an HMG-CoA reductase inhibitor, and more particularly Fluvastatin, Atorvastatin or salts thereof in combination with a linear sulphated polysaccharide such as Carrageenan and a method for the preparation thereof.
CN102872096A Application of Houttuynoid E in medicine for treating lung cancer The invention discloses application of Houttuynoid E in preparing a medicine for treating lung cancer. The compound shows high anti-lung cancer activity and can be used for preparing an anti-lung cancer medicine, belonging to the technical field of new application of a medicine. The Houttuynoid E can obviously suppress the non-small cell lung cancer cell A549, large cell lung cancer cell NCI-H460, squamous cell lung cancer cell HTB-8 and human lung squamous epithelium cancer cell QG-5 cultured in vitro while realizing a relatively low effect on suppressing the human normal liver cell LO2 and peripheral blood lymphocyte cell, thereby showing obvious selectivity. The application of Houttuynoid E in preparing a medicine for treating lung cancer is disclosed for the first time; and the skeleton type is a brand new one, and the activity in suppressing lung cancer cells is unexpectedly strong.
CN101991587A Compound sulfadiazine injection and preparation method thereof The invention discloses a compound sulfadiazine injection and a preparation method thereof. The compound injection comprises the following components in parts by weight: 5-12 parts of sulfamonomethoxine sodium, 1-5 parts of trimethoprim (TMP), 0.1-0.3 part of anhydrous sodium sulfite, 0.01-0.05 part of disodium ethylene diamine tetraacetate, 8-10 parts of sulfamethoxazole, 20-50 parts of propylene glycol, 1-5 parts of ethanolamine and 45-79 parts of injection water. Compared with the single sulfamonomethoxine sodium, the compound preparation prepared from the sulfamonomethoxine sodium, the sulfamethoxazole and the TMP expands an antibacterial spectrum, enhances the curative effect of the injection and enlarges the clinical application range; and the compound preparation can be applied to treating infection caused by bacteria as well as fever, high fever and dyspnea caused by toxoplasma, and the preparation has better treatment effect on diseases such as appetite decrease and even anorexia, diarrhea and the like.
CN101015355A Preparing method of squid melanin iron and application thereof The invention discloses a method for preparing squid melanin-Fe. It is characterized in that it comprises following steps: separating melanin from squid ink, putting it into Fe- containing solution after vacuum freeze-drying, adjusting pH to 3-6 with acid, stirring for 8-24 hours under 4- 25 Deg. C, collecting depositions after 3000-5000Xg centrifugation at room temperature; washing the depositions repeatedly with distilled water, collecting depositions after 3000-5000Xg centrifugation, then freeze-drying in vacuum condition. The squid melanin-Fe is useful for preparing adjuvant treatmenthealth foods, functional foods or drugs. The invention takes sea squid ink as raw material, then puts Fe ion into high- purity squid melanin to prepare squid melanin-Fe. It is characterized by abundant raw material, high- content melanin, simple steps, fewer equipment investment, no pollution, high yield, and suitability for industrial production.
CN103330685A Cefaclor granule and preparation method thereof The invention discloses a cefaclor granule and a preparation method thereof. The cefaclor granule is prepared by mixing a cefaclor granule clathrate compound with pharmaceutically acceptable auxiliary materials. The cefaclor granule clathrate compound is prepared by following steps: dissolving polyvinyl alcohol-polyethylene glycol graft copolymer (Kollicoat IR) in ethanol; adding cefaclor in the solution; and keeping stirring the solution and removing ethanol by vacuum drying method so as to obtain the cefaclor granule clathrate compound. Stability and dissolution rate of the cefaclor granule are high, production technology is simple, and the cefaclor granule is suitable for industrial production.
CN103120747A Drug for treating vital myocarditis The invention discloses a drug for treating vital myocarditis, and the drug is prepared from the following raw materials in parts by weight: 10-15 parts of radix isatidis, 8-12 parts of folium isatidis, 2-6 parts of ginseng, 6-10 parts of radix salviae miltiorrhizae, 8-12 parts of radix astragali, 2-3 parts of honeysuckle flowers, 2-4 parts of pseudo-ginseng, 3-6 parts of poria with hostwood, 5-13 parts of platycladi seeds, 5-13 parts of radix asparagi, 4-8 parts of leeches, 2-4 parts of rhizoma ligustici wallichii, 5-13 parts of fructus schizandrae, 3-12 parts of liquorice, 3-6 parts of polygala tenuifolia and 1-2 parts of cinnabar and also contains cinnamaldehyde, creatinine, a vitamin C, coenzyme Q10, and the like. The drug disclosed by the invention combines the traditional and Western medicine, can be used for treating both symptoms and root causes, has the effects of diminishing inflammation and resisting viruses, tonifying Qi and replenishing blood, nourishing yin and clearing heat, nourishing heart and calming nerves, eliminating evil and strengthening healthy energy and can be used for treating palpitation, short breath, heart meridian disorder, chest distress, asthenia, spontaneous perspiration, limb and mind fatigue, precordial pain, severe palpitation and intermittent pulse. After the drug disclosed by the invention is taken by a patient, an ideal treatment effect is achieved, and the myocarditis symptoms are obviously improved or eliminated.
WO2007039782A1 Tetrazole derivatives as modulators of metabotropic glutamate receptors The present invention relates to new compounds of formula (I) wherein Y1 and Y2 selected from the group consisting of hydrogen, halogen atom, C1-4 alkyl, C1-4 alkoxy or cyano group, X is oxygen or two hydrogen atoms; Z is -(CH2)n- group or S; n is 1 or 2; R is selected from the group consisting of optionally substituted C1-7 alkyl, C1-4 haloalkyl, C1-4 hydroxyalkyl, C1-3OC1-3 alkyl, C1-4 cyanoalkyl, C0-2(NR1R2)alkyl, C1-4-alkylCOOC1-4-alkyl, C1-4-alkylOCOC1-4-alkyl, C1-4-alkylNHCOC1-4-alkyl, C2-7 alkenyl, C2-7 alkynyl, CH2O-(CH2)1-3-OCH3; an optionally substituted C3-7 cycloalkyl; phenyl; C3-7 saturated or unsaturated heterocyclyl or heteroaryl group containing 1-4 heteroatom; R1 and R2 are independently selected from hydrogen, C1-7 alkyl or C1-6 alkanoyl group - and/or enantiomers and/or racemates and/or diastereomers and/or geometric isomers and/or pharmaceutically acceptable salts thereof formed with acids and bases, to the process for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
CN101214251A Pennogenyl saponins compounds percutaneously absorbable preparation The present invention relates to a special preparation form, in which, pennogenyl saponin compound is considered as active component. A percutaneous absorption preparation of the pennogenyl saponin compound of the present invention consists of the components with the following weight percentage of 0.05 percent to 40 percent of the pennogenyl saponin compound, 1 percent to 20 percent of penetration accelerant and 40 percent to 98.5 percent of medical matrix. The activity of the pennogenyl saponin compound of the present invention is very strong, the daily dosage is only 1 to 10mg, and only 5 percent to 10 percent of absorption into blood can act, which is very fit for manufacturing a percutaneous preparation. The medication time of the percutaneous preparation can be controlled freely by a patient, which can not cause the bad reaction in gastrointestinal tract. Because of the difference of the medical matrix, the percutaneous preparation of the pennogenyl saponin compound can be made into ointment preparation, cataplasm, coating agent and aerosol.
CN102526666A Ginger-long pepper composition of for reducing vomit caused by cancer chemotherapy and enhancing chemotherapy and preparation method thereof The invention relates to a natural medicinal composition, a preparation method thereof and an application of the natural medicinal composition to preparation of a detoxifying and enhancing medicament used in cancer chemotherapy. The natural medicinal composition consists of a ginger-long pepper decoction concentrated extract, gingerol, a long pepper ethanol extract and piperine in the ratio of (2-8):(1-4):(2-4):(3-9). The composition has extremely good curative effects on side effects such as vomit and the like caused by cancer chemotherapy, and can play a role in inhibiting tumors simultaneously.
US20050215584 Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which α7 is known to be involved.
US20080138385 2-mercaptopyridine-N-oxide sodium, carbendazim (methyl 1H-2-benzimidazole carbamate), or thiabendazole (2-(4-thiazolyl)-1H-benzimidazole); halogen-free; synergistic effect An antibacterial composition containing an organic antibacterial agent and an inorganic antibacterial agent is provided. Zirconium phosphate having supported thereon silver or copper or a salt thereof may be used as the inorganic antibacterial agent, and 2-mercaptopyridine-N-oxide sodium, carbendazim (methyl 1H-2-benzimidazole carbamate), or thiabendazole (2-(4-thiazolyl)-1H-benzimidazole) may be used as the organic antibacterial agent. Those components contain no halogen, so the antibacterial composition can be made halogen-free. The antibacterial composition may be applied to form an antibacterial molding, for example, by molding it together with a resin material or applying it together with a coating agent on a resin molding.
WO2010065159A1 Inhibition of dna polymerases to augment chemotherapeutic and antimicrobial agents Disclosed herein is the identification of human DNA polymerase K (pol K) as the polymerase that mediates repair of DNA containing interstrand crosslinks (ICLs). The mechanism of action of a number of chemotherapeutic and antimicrobial agents is the induction of ICLs. Thus, provided herein is a method of enhancing the efficacy of a chemotherapeutic or antimicrobial agent in a subject, including selecting a subject in need of treatment with an ICL-inducing agent and administering to the subject an ICL-inducing agent and a therapeutically effective amount of an inhibitor of pol K. Subjects in need of treatment with an ICL-inducing agent, include, for example, subjects diagnosed with a hyperproliferative disease, an autoimmune disease or an infectious disease. Also provided is a composition for treating a hyperproliferative disease, an autoimmune disease or an infectious disease, comprising an ICL-inducing agent and an amount of an inhibitor of pol K sufficient to enhance the efficacy of the ICL-inducing agent. Further provided is a method of identifying a DNA polymerase inhibitor.
CN103393779A External medicine for treating rosacea The invention relates to an external medicine for treating rosacea. A preparation method of the external medicine which is ointment comprises crushing 10-25 weight parts of coptis, 5-15 weight parts of calomel, 3-8 weight parts of mercury, 30-55 weight parts of walnut meat, 40-55 weight parts of calamine, 20-30 weight parts of natural indigo and 8-15 weight parts of Hainan chaulmoogra seed, sieving the powder by a sieve of 140 meshes, adding leaf fat into the sieved powder, blending the mixture into a paste, and carrying out sterilization by high pressure steam. The external medicine has the advantages of good treatment effects, fast treatment, no irritation and no adverse reaction.
WO2007055418A1 Aza-substituted spiro derivative Disclosed is a compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. [In the formula, X, Y, Z and W independently represent a methine group or a nitrogen atom, but all X, Y, Z and W are not methine groups at the same time; A represents -O- or the like; B represents -C(O)- or the like; D represents -(CH2)m2-, -O- or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1): (Wherein R6, R7 and R8 independently represent a lower alkyl group or the like).]
WO2013054862A1 Polycyclic pyridone derivative having integrase-inhibiting activity The present invention relates to a compound represented by formula (I-1), formula (I-2), or formula (I-3) having an antiviral effect, or a pharmaceutically acceptable salt thereof, and in further detail, to a pyridone derivative having HIV integrase-inhibiting activity and a drug, particularly an anti-HIV drug, containing the derivative. The compound of the present invention has integrase-inhibiting activity and/or cell propagation-inhibiting activity against a virus, particularly HIV or a resistant virus thereof. Thus, the compound of the present invention is useful in the prevention or treatment of a variety of illnesses and viral infections (such as AIDS) in which integrase plays a role. (Each symbol in the formulas is as defined in the Specification.)
WO2006076568A3 Thiazolopyridines as cannabinoid receptor modulators The present application describes compounds according to Formula (I), pharmaceutical compositions comprising at least one compound according to Formula (I) and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula (I) both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula (I): including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R3a, R4, A, B, and n are described herein.
US20090041828 Insert for the treatment of dry eye The invention relates to an insert for the treatment of dry eyes, wherein the insert can be placed on or inserted into the lacrimal sac or the cornea.
CN101785780A Preparation of cyanocobalamine and adenosine composition and preparation method thereof The invention relates to the field of the pharmaceutical preparation, in particular to a cyanocobalamine and adenosine combined pharmaceutical preparation, and comprises an oral solid preparation, injection, a freeze-dried preparation for injection and a preparation method thereof. Each unit of pharmaceutical preparation of the invention comprises 0.05-5.0mg of cyanocobalamine and 0.05-5.0mg of adenosine, wherein the weight ratio of the cyanocobalamine and the adenosine is 1:10-10:1, and the preferential weight ratio is 1:5-5:1.
US8071616 Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.
CN102415996A Valnemulin hydrochloride self-emulsified oral nano emulsion for veterinary use and preparation method thereof The invention discloses valnemulin hydrochloride self-emulsified oral nano emulsion for veterinary use and a preparation method thereof. The valnemulin hydrochloride self-emulsified oral nano emulsion for veterinary use comprises the following components: valnemulin hydrochloride, oil, surfactant, preservative, antioxygen and auxiliary surfactant. After disintegrating in water and being stirred slightly or being taken orally and moving with intestine movement, the self-emulsified emulsion can spontaneously form emulsion with emulsion droplet size of 10 to 100 nanometers; the drawbacks of decomposition of valnemulin during long standing and content reduction of the valnemulin or valnemulin hydrochloride nano emulsion prepared in the prior art are overcome and the content stability of the product is increased; the palatability of the valnemulin product is improved; and the preparation process is simple, and the valnemulin hydrochloride self-emulsified oral nano emulsion is suitable to be produced in large scale by veterinary medicine enterprises.
WO2005056056A3 The combination of a serotonin reuptake inhibitor and a histamine 3 receptor antagonist, inverse agonist or partial agonist The invention relates to the use of a compound, which is a serotonin reuptake inhibitor, and another compound, which is a H3 receptor antagonist, inverse agonist or partial agonist for the preparation of a pharmaceutical composition for the treatment of depression, anxiety disorders and other affective disorders, such as generalized anxiety disorder, panic anxiety, obsessive compulsive disorder, acute stress disorder, post traumatic stress disorder and social anxiety disorder, eating disorders such as bulimia, anorexia and obesity, phobias, dysthymia, premenstrual syndrome, cognitive disorders, impulse control disorders, attention deficit hyperactivity disorder, drug abuse or any other disorder responsive to serotonin reuptake inhibitor.
CN102827135A Compound for preparing medicine for treating avian influenza and preparation method of compound The invention discloses a compound (E)-3-(5-(1-acetoxyl-2-oxoethyl)-2, 2-dimethyl-1, 3-dioxacyclopentyl-4-yl ethyl acrylate (with structural formula shown as the formula I) for preparing a medicine for treating avian influenza, and a preparation method of the compound. The compound disclosed by the invention can be served as an intermediate for a series of carbocyclic compound which has activity to resist avian influenza; and the preparation method is environment-friendly, simple in technology, and low in cost, and the average yield is 40%.
US20090181040 Triazinone compounds for treating diseases resulting from infestation with parasitic protozoans The present invention relates to the use of triazinones such as triazinediones and triazinetriones for triazinetriones for the preparation of compositions for treating animals, in particular treating animals prophylactically, against parasitic protozoans, and to these compositions.
WO2006080327A1 ANTICANCER DRUG CONTAINING α,α,α-TRIFLUOROTHYMIDINE AND THYMIDINE PHOSPHORYLASE INHIBITOR A drug for cancer treatment enhanced in efficacy and safety. There is provided a drug for cancer treatment comprised of a composition containing α,α,α-trifluorothymidine (FTD) and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5. The drug for cancer treatment is orally administered in a dosage of 20 to 80 mg/m2/day in terms of FTD, the dosage divided and given two to four times each day.
US7883713 Suspension, ointment, solution, spray, lotion, gel, cream, powder, powder spray, paste, emulsion, foam or stick; for treatment of herpes infections in humans The invention relates to the topical application of substituted thiazolyl amides in the treatment of herpes infections in humans, to preparations suitable for the topical application and to the production thereof.
US20100331383 Compounds for the treatment of aids and other viral diseases The present invention provides methods for treating Acquired Immunodeficiency Syndrome (AIDS) and other viral diseases and Human Immunodeficiency Virus (HIV) related infections by administering one or more compounds of formula I: wherein: the dotted line represents a single or a double bond; and R1 and R2 are the same or different and independently of each other represent —CH2OH, —CH2OR4, —CH(OH)CH3, —CH(OR4)CH3 or a group represented by the formula: or salts or hydrates thereof in a carrier which minimizes micellar formation or van der Waals attraction of molecules of said compound. The invention also provides S enantiomeric forms of such compounds which possess the ability to inhibit cell growth whilst being of low toxicity to such cells and methods of making such compounds.
US7101885 1-(4-Bromo-phenyl)-3-[2-(4-methyl-piperazin-1-yl)-pyridin-3-yloxy]-pyrrolidin-2-one; antagonists of the serotonin 5HT1B receptor; treating depression The present invention relates to compounds of formula I wherein Ar, Y and G are as defined in the specification, a is 1 to 4, Z and W are carbon or nitrogen and n is 1, 2 or 3; and to pharmaceutical compositions comprising the compound of formula I and a pharmaceutically effective carrier; and to a method useful in treating or preventing in mammals, including humans, a disorder or condition selected from the group consisting of anxiety, depression, dysthymia, major depressive disorder, migraine, post-traumatic stress disorder, avoidant personality disorder, borderline personality disorder and phobias.
US20090202611 Composite self-cohered web materials The present invention is directed to implantable bioabsorbable non-woven self-cohered web materials having a high degree of porosity. The web materials are very supple and soft, while exhibiting proportionally increased mechanical strength in one or more directions. The web materials often possess a high degree of loft. The web materials can be formed into a variety of shapes and forms suitable for use as implantable medical devices or components thereof.
US7585867 Substituted thiazolo[4,5-d]pyrimidin-2(3H)-one A compound of formula (I) and pharmaceutically acceptable salts or solvates thereof for use in therapy.
CN103417690A Colon-cleansing drug used before urinary endoscopic surgery The invention discloses a colon-cleansing drug used before urinary endoscopic surgery and aims to solve the problem of treatment before urinary endoscopic surgery. The colon-cleansing drug is characterized by being prepared by the following active pharmaceutical ingredients, by weight proportion, horseweed herb, fructus cinnamomi, radix ranunculi ternati, Chinese starjasmine stem, clausena excavata burm, mulberry, dipsacus roots, tangerine peel, sunflower flowers, turbo cornutus solander, amblystegium serpens and magnesium sulfate. Clinical experiments show that the colon-cleansing drug has good colon-cleansing effect when used before urinary endoscopic surgery, and is worthy of clinical application and popularization.
WO2008093247A3 Medicament for the treatment of endometriosis The use of a dopamine agonist in the manufacture of a medicament for the treatment or prevention of endometriosis.
CN102977107A Pemetrexed disodium compound and composition thereof The invention discloses a pemetrexed disodium compound expressed by the formula (I) and a composition thereof, wherein the pemetrexed disodium compound is measured by powder X-ray diffractometry so that the X-ray powder diffraction pattern expressed by the diffraction angle of 2theta+/-0.2 of the compound shows feature diffraction peaks at 10.05 degrees, 10.90 degrees, 11.40 degrees, 12.51 degrees, 14.22 degrees, 15.94 degrees, 18.33 degrees, 19.72 degrees, 21.44 degrees, 22.92 degrees, 23.84 degrees, 28.08 degrees, 29.98 degrees, 31.95 degrees and 33.32 degrees. The pemetrexed disodium compound provided by the invention is obviously improved in stability, low in organic solvent residual volume, controllable in quality, and not easy to change even though being placed for a long time; therefore, the medication safety of the patient is greatly improved.
WO2007143066A2 Method for predicting susceptibility to radiation pneumonitis Provided is a method for determining whether an individual is likely to be susceptible to radiation pneumonitis from radiation therapy and for developing a treatment based on the determination of susceptibility. The method involves measuring SOD and GPX activity levels. A high SOD or low GPX activity, or a combination thereof, is indicative that the individual is likely to be susceptible to radiation pneumonitis.
CN101143136A Paroxetine slow release micropills preparation The invention relates to a preparation, which contains paroxetine or the medicinal applicable salt and the application of the preparation for remedying and/or preventing certain diseases. The invention provides a paroxetine slow-release pellet preparation which contains polymeric slow-release combinations, including paroxetine tablet core with curative treatment dosage and/or protective dosage and the pellet which is applied in the tablet core and partially covers the surface of the tablet core and is slowly dissolved inside the liquid with water. The invention solves the clinical application problem of the prior paroxetine slow-release preparation. The invention also provides the applications of the paroxetine slow-release pellet preparation for preparing the drugs for remedying and/or preventing various types of depressions and reducing various kinds of diseases which are caused by mental factors.
WO2013192088A1 SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy,Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
US20050037955 Bactericides; fungicides; isolated polypeptides; inflammatory bowel disorders; infections The present invention relates to microbial (antibacterial and antifungal) and other therapeutic treatments for diseases, in particular but not limited to the intestine, based upon angiogenins, and particularly angiogenin-4: a novel intestine-specific, epithelial-based, microbially-regulated member of the angiogenin family. Novel proteins as well as their use in screening for pharmaceuticals are also described.
US20090312383 Fused Heterocyclic Compounds There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or —NR3— (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, —CO—, oxygen, sulfur, —SO—, —SO2—, —NR4—, —NR4-alk-, —CONR4— or —NR4CO— (wherein alk is an optionally substituted C1-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.
WO2008072535A1 Pharmaceutical composition containing low-substituted hydroxypropylcellulose Disclosed is a pharmaceutical composition containing a compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof, while having improved dissolvability. Specifically disclosed is a pharmaceutical composition containing (A) a compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof, and (B) a low-substituted hydroxypropylcellulose.
US7718795 Succinoylamino benzodiazepines as inhibitors of aβ protein production This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
EP1165534B1 Benzoylguanidine derivatives with advantageous properties, method for producing them and their use in the production of medicaments The invention relates to novel benzoylguanidine derivatives of general formula (I), to a method for producing them and to their use in the production of medicaments.
CN1748685A Oxidendazole nasal jelly for treating nasal polyp and nasal polyp diseases The present invention relates to the preparation process of nasal oxibendazole jelly and the application of the nasal oxibendazole jelly in treating nasal polyp and nasal polyp disease and in preventing recurrence of polyp after surgical operation treatment, laser treatment and other treatment.
EP1737864A1 Selected cgrp antagonists, methods for the production thereof, and use thereof as medicaments The invention relates to the CGRP antagonists of general formula (I), wherein A and R1 to R3 are defined as indicated in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof, the hydrates of the salts, especially the physiologically acceptable salts thereof with inorganic or organic acids, medicaments containing said compounds, the use thereof, and methods for the production thereof.
US20060251663 Employment of rotavirus proteins, derived proteins and peptides for the modulation of tisssue permeability The present invetnion refers to the use of rotavirus proteins VP4, VP8 and their derived fusion proteins and peptides, for enhancing the delivery of pharmaceutical agents through the paracellular pathway. These rotavirus proteins and derived peptides may additionally be employed to reduce unwanted cellular adhesion that can occur between cancerous cells, or between normal cells as a result of surgery, injury, chemotherapy, disease, inflammation or other pathological conditions.
WO2008020596A2 Treating or preventing cancers over-expressing reg4 or kiaa0101 The invention features a method for inhibiting growth of a cancer cell by contacting the cell with a composition of an siRNA that inhibits expression of REG4 or KIAA0101. Methods of treating cancer are also within the invention. The invention also features products, including nucleic acid sequences and vectors as well as to compositions comprising them, useful in the provided methods. The invention also provides a method for inhibiting of tumor cell, for example pancreatic cancer cell, prostatic cancer cell, breast cancer cell, and bladder cancer cell, particularly pancreatic ductal adenocarcinoma (PDAC) by inhibiting REG4 gene. The present invention also relates to methods of treating or preventing PDAC in a subject comprising the step of administering to said subject a pharmaceutically effective amount of an antibody or fragment thereof that binds to a protein encoded by REG4. The present invention also relates to methods of diagnosing chemo-radiation therapeutic resistance of a cancer. The present invention also provides therapeutic agents or methods for treating cancer using the polypeptides. The polypeptides of the present invention are composed of an amino acid sequence which comprises polypeptide which comprises QKGIGEFF/SEQ ID NO: 21. The polypeptides of the present invention can be introduced into cancer cells by modifying the polypeptides with transfection agents such as poly-arginine.
US8106181 Methods for producing interfering RNA molecules in mammalian cells and therapeutic uses for such molecules Methods for producing interfering RNA molecules in mammalian cells are provided. Therapeutic uses for the expressed molecules, including inhibiting expression of HIV, are also provided.
US6964962 A norepinephrine reuptake inhibitor or its salt and a neuroleptic agent A composition comprising: (a) a pharmaceutically effective amount of reboxetine; and selected from the group consisting of clozapine, olanzapine, risperidone and mixtures thereof (b) a pharmaceutically effective amount of one or more neuroleptic agents or a pharmaceutically effective salt thereof is provided.
US20120134950 Adhesion-Promoting thin Film and Moisture Resistant Skin Barrier Compositions Adhesion-promoting, thin film, moisture resistant skin barrier formulations are composed of a fugitive solvent mixture consisting of t-butanol and an alkane fraction composed of at least one alkane, where the t-butanol is in the range of 40-70% by weight of the solvent mixture, and a film-forming solute dissolved in the fugitive solvent mixture. The formulations may also include one or more optional ingredients such as antimicrobial and/or bioactive agents. When applied to the skin, the formulations improve the adhesion of various classes of medical adhesives used to attach a variety of medical devices to the skin and create a thin, flexible and elastic continuous barrier film on the skin to protect against body fluids and incontinence.
CN103432092A Sustained release preparation of repaglinide The invention relates to a sustained release preparation of repaglinide, and a preparation method and an analysis method of the sustained release preparation. The sustained release preparation comprises the components: hydroxypropyl methyl cellulose, ethylcellulose, acrylic resin, poloxamer, sodium carboxymethylcellulose, polyethylene glycol and the like serving as slow release materials.
US7189383 Compounds with halogen for diagnosis with ethers or sulfides for cancer The present invention relates to Halogenated amino acid analogues for use in diagnosis, which compounds have the general formula (I) wherein: R is (C1–C6) alkyl optionally substituted with thioether or ether oxygen atom when n=0, or a substituted aromatic or heteraromatic ring when n=1–6; and m=0 or 1; and X is a halogen atom. The invention further relates to precursor compounds for these analogues, to a method of preparing these analogues, to a pharmaceutical composition comprising these analogues and to the use of these analogues and compositions in the diagnosis of cancer
WO2010052896A1 Preparation for local administration containing fluticasone propionate Fluticasone propionate microparticles useful as active ingredients for a preparation for local administration which enables the long-term retention of microparticles of an active ingredient in a mucosa for a long period to achieve a higher therapeutic effect and a higher long-acting property, each of which comprises a fluticasone propionate crystal core and needle-like fluticasone propionate crystals which have been grown radially around the crystal core and which has an average particle size of 10 to 60 μm.
EP1853232A1 Stable crystalline form of bifeprunox mesylate, dosage forms thereof adn methods for using them The present disclosure provides novel pharmaceutical compounds and methods for making the same, novel pharmaceutical dosage forms and methods for making the same, and the use of said compounds and dosage forms for the manufacture of a composition to treat and prevent diseases and/or disorders.
CN1723914A Compound medicine contg. heparin zinc, and its application A composite medicine containing heparin zinc in the form of cream, ointment, gel, powder, filming agent, etc for treating scald is prepared proportionally from heparin zinc, a polysaccharide chosen from hyaluronate, chondroitin sulfate salt and alginate.
WO2007037333A1 Inhibitor of binding to non-typical proline-rich sequence Disclosed is an inhibitor of the binding to a non-typical praline-rich sequence, which comprises a non-peptidic compound or a pharmacologically acceptable salt thereof as an active ingredient. The inhibitor comprises, as an active ingredient, a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof: (I) wherein R1, R2, R3A, R3B, R4, R5A, R5B, R6, R7, R8, R9A and R9B are as defined in the description.
WO2009138198A3 Compositions comprising hydroxytyrosol for the preventive and curative treatment of intestinal tract disorders Disclosed are oral compositions with enhanced release in the intestinal tract which contain hydroxytyrosol as active ingredient, and possibly a soluble dietary fibre.
WO2007076127A3 Condensed imidazoles or pyrazoles and their use as transforming growth factor modulators The invention relates to compounds of formula I that are modulators of Transforming Growth Factor β (TGF β) and are useful for treating TGF β related diseases. In Formula (I) one of Rl or R2 is heteroaryl and the other is aryl or heteroaryl, one of Xl or X2 is C and the other is N.
WO2009104150A1 Combination comprising bosentan for treating ovarian cancer The invention relates to the combination of bosentan with paclitaxel, and in particular to this combination for therapeutic use, simultaneously, separately or over a period of time, in the treatment of ovarian cancer.
US20100209484 Transdermal Triptan Delivery System This invention relates to transdermal system for the systemic administration of an active ingredient such as a triptan selected from the group comprising eletriptan, frovatriptan, sumatriptan, zolmitriptan, naratriptan, rizatriptan and almotriptan uniformly over periods of 12 to 24 hours or more thereby reducing the probability of recurring migraine. The formulation includes active ingredient, adhesive matrix and permeation enhancer. The invention also relates to storage stable formulations and methods for preventing migraine and cessation of an ongoing migraine event.
US20110200673 Oxidized heparin fractions and their use in inhibiting angiogenesis The present invention relates to a heparin fraction comprising constituents having molecular weights of from about 2,000 to about 4,000 daltons, wherein from about 1% to about 100% of hydroxyl residues of the constituents are oxidized. The present invention also relates to methods of inhibiting angiogenesis and treating an angiogenesis-mediated disorder in a subject by administering a heparin fraction comprising constituents having molecular weights of from about 2,000 to about 30,000 daltons, wherein from about 1% to about 100% of hydroxyl residues of the constituents are oxidized. Another aspect of the present invention relates to compositions including the heparin fractions of the present invention.
WO2006040676A1 Nitrosated benzopyran compounds as novel cyclooxygenase-2 selective inhibitors This invention specifically relates to novel cyclooxygenase 2 (COX-2) selective inhibitor compounds that donate, transfer or release nitric oxide, stimulate endogenous synthesis of nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase. Compounds of particular interest and their analogs defined by formula (I) wherein Z, X, R1, R2, R3, and R4 are as described in the specification. This invention also relates to pharmaceutical compositions and methods for treating COX-2 mediated disorders, such as inflammation and inflammation related disorders.
CN100594214C Substituted oxazolobenzoisothiazole dioxide derivatives, production method and use thereof The invention relates to compounds of formula (I), where the groups have the given meanings and the physiologically-acceptable salts thereof. The compounds are suitable as medicaments for lowering blood sugar levels and for prevention and treatment of diabetes.
CN101347438A Medicament for slowing down angiogenesis of eye section The invention relates to an application of a steroid compound to a medicine for inhibiting the generation of ocular neovascularization. The preparation of preparations related to the medicine is also related.
US20110293694 Quantum unit of inheritance vector therapy method The innovative treatment method described here utilizes configurable microscopic medical payload delivery devices to act as a transport vector to deliver quantum genes to specific type of cells in the body. Utilizing probes on the exterior of the transport device, transport device locate specific target cell types in the body. Once a specific target cell type has been encountered, the configurable microscopic medical payload delivery device inserts its payload of quantum genes into the target cell type. By delivering quantum genes to specific type of cells, genes can be activated or inactivated in those specific type of cells. This method of delivering medically therapeutic quantum genes to specific cells is intended to improve cell function or extend the longevity of cells or neutralize harmful cells that pose a hazard to the body.
CN103372179A Plaster preparation for relieving pain, activating blood, softening hard mass and removing blood stasis, and preparation method thereof The invention discloses a plaster preparation for relieving pain, activating blood, softening hard mass and removing blood stasis, and a preparation method thereof. The plaster preparation comprises the following components in parts by weight: 60-70 parts of black medicine meat, 4-6 parts of raw salted aconite root, 10-15 parts of cortex cinnamomi, 20-25 parts of pepper and ginger powder, 18-22 parts of radix angelicae, 4-6 parts of pepper, 8-12 parts of rhizoma kaempferiae, 2-4 parts of as arum, 4-6 parts of musk or menthol, and 3-4 parts of borneol. The plaster preparation is available in materials, simple to prepare, and low in cost; the plaster is fast to take effect, high in curative effect and free of side effect; the recovery rate can be up to over 95%.
CA2601000A1 Arylsulfonyl benzofused heterocycles as 5-ht2a antagonists Compounds of formula (I): are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various CNS disorders.
US20090076160 Use of R (+) -N-propargyl-1-aminoindan to treat or prevent hearing loss A method of treating or inhibiting hearing loss in a mammalian subject, comprising administering to the subject an amount of R(+)-N-propargyl-1-aminoindan or pharmaceutically acceptable salt thereof effective to treat or inhibit the hearing loss in the subject.
WO2008119176A1 Amidation process for the preparation of cathepsin k inhibitors This invention describes an amidation process whereby amino acids of the Formulae IIA or IIB can be activated and treated with an amine in the presence of a base to yield amides of the Formula (I), without loss of optical purity.
CA2832886A1 Polymer conjugated prostaglandin analogues The present invention relates in general to polymer-drug conjugates. In particular, the invention relates to polymer-drug conjugates wherein the conjugated drugs are selected from prostaglandins and substituted prostaglandins, to a method of delivering such prostaglandin drugs to a subject, to a sustained drug delivery system comprising the polymer-drug conjugates, to a method of preparing the polymer-drug conjugates, and to an implant comprising the polymer-drug conjugates. The polymer-drug conjugates may be useful for delivering prostaglandins and substituted prostaglandins for the treatment of glaucoma.
US20110015277 Method of producing egg yolk based functional food product and products obtainable thereby The present invention relates to the field of food products, especially food products specifically designed for providing health benefits beyond the basic function of nutrition for a subject consuming the product on a regular basis, e.g. on a daily basis. According to the present invention eggs are produced, in particular chicken eggs, that are enriched in one or more pharmacologically active nutrients. The egg yolk obtained from the aforementioned eggs can suitably be used in high amounts as a component of a functional food product having all the characteristics that are normally required for such functional food products. A preferred example of a food product in accordance with the invention is a ready to drink shot containing approximately one whole egg yolk in a volume as small as 100 ml.
US20120129924 Uses of sesquiterpene derivatives The present invention relates to a pharmaceutical composition for preventing or treating hyperlipidemia, fatty liver, diabetes and obesity comprising a sesquiterpene derivative as an active ingredient. The sesquiterpene derivatives of the present invention leads to decrease in body fat weight, visceral fat weight and total cholesterol levels, triglyceride of plasma and liver tissue, blood glucose and blood insulin levels in a fast state, finally exhibiting efficacies on prevention or treatment of hyperlipidemia, fatty liver, diabetes and obesity.
US6974800 Formulations comprising an inhibitor of carboxypeptidase U and A thrombin inhibitor The present invention relates to pharmaceutical formulations of an inhibitor of carboxypeptidase U (CPU) and a thrombin inhibitor in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, as well as a kit of parts, a method for treatment and use of the formulations for the treatment of a condition in which inhibition of CPU and/or inhibition of thrombin are required or desired.
WO2014021273A1 Morphinan derivatives The morphinan derivatives represented by general formula (I) (wherein: R1 represents a cycloalkyl alkyl, an aralkyl, or the like; R2 represents an aralkyl, a heteroaryl alkyl, or the like; R3, R4 and R5 represent hydrogen, a hydroxy, or the like; R6 and R7 represent hydrogen or the like; R8 and R9 represent hydrogen or the like; X represents O or CH2; and Y represents a bond or the like), tautomers and stereoisomers of said compounds, or pharmaceutically acceptable salts or solvates thereof are used as analgesics, antidepressants, and anxiolytics.
CN103211802A Novel application of phloroglucinol The invention discloses a novel application of phloroglucinol, namely an application of phloroglucinol in preparing medicaments for treating bronchial asthma or chronic cough. The new application provides a new treatment way for patients with bronchial asthma and chronic cough; the phloroglucinol is used for relieving or treating the bronchial asthma and chronic cough diseases and obviously improving the cough, expectoration and asthma symptoms of the patients, has the advantages of no toxic and side effects, good treatment effect and the like, and is easily accepted by the patients.
WO2009101812A1 Glutamic acid transporter inhibitor Disclosed is an excellent glutamic acid transporter inhibitor. Specifically disclosed is a glutamic acid transporter inhibitor which contains a diphenylbutene derivative represented by general formula (1) or a salt thereof as an active ingredient. [In the formula, R1 and R2 may be the same or different and each represents a hydrogen atom, a hydroxy group, a halogen atom, a carboxy group, an alkyl group which may be substituted by a halogen atom or a hydroxy group, or an alkoxy group which may be substituted by a halogen atom, a dialkylamino group or a five-membered or six-membered saturated heterocyclic group containing at least one nitrogen atom; and two R3's represent the same groups which are hydrogen atoms, alkyl groups or phenyl groups.]
WO2014052415A3 Measurement of brain cdp-diacylglycerol synthase 1 enzyme and uses thereof Provided herein are methods of diagnosing depressive disorders in a subject by comparing a CDP-diacylglycerol synthase 1 enzyme activity or expression level to enzyme activity or expression level of CDP-diacylglycerol synthase 1 in a control subject. Also herein are methods of predicting therapeutic efficacy of an antidepressant drug in a subject with depressive disorders by monitoring enzyme activity or expression level of CDP-diacylglycerol synthase 1 in the subject. Further provided herein are methods of identifying a compound effective to treat or alleviate the symptoms of depression by monitoring enzyme activity or expression level of CDP-diacylglycerol synthase 1 in a tissue. Further provided are kits for diagnosing depressive disorders.
EP2373998A1 Nitroprotein biomarkers for copd The invention relates to the use of specific nitroprotein biomarkers as prognostic and diagnostic tools for COPD. Identification of certain specific nitroprotein biomarkers allows the development of targeted therapies aimed at prevention and treatment of COPD.
US20050261330 Derivatives of 2,2,4-trisubstituted tetrahydrofuran an antifungal agents The present invention relates to derivatives of 2,2,4-trisubstituted tetrahydrofuran as potential antifungal agents. This invention also relates to pharmaceutical compositions containing the compounds of the present invention and their use in treating and/or preventing the fungal infections in mammals, preferably humans.
WO2006122408A1 Bir domain binding compounds The present invention is directed towards an isomer, an enantiomer, a diastereoisomer, or a tautomer of a pyrrolidine compound represented by Formula (I) in which the substituents R1, R1a, R2, R2a, R3, A and Q are defined herein; or a prodrug, or a salt thereof, and which bind to IAP BIR domains. In particular, the compounds are useful in treating proliferative disorders such as cancer.
WO2012111795A1 Ameliorating agent for lifestyle-related diseases containing water extract of colored onion Provided is a PPARγ activator which contains, as an active ingredient, a water extract of a colored onion that contains 70 mg or more of quercetin glycoside per 100 g of the fresh edible part in weight. A pharmaceutical product, food and drink each containing the PPARγ activator are useful for prophylaxis, treatment or amelioration of lifestyle-related diseases, metabolic syndrome, menopausal disorders and osteoporosis.
WO2008052288A1 Dithiole compounds as cox inhibitors A compound of formula (I) wherein: R1 and R2 are the same or different and are independently selected from H and a shielding group; X and Y are each independently selected from N and CH; R3 is hydroxy, alkoxy, acyloxy or an ester group; R4 is a direct bond to R5, -CH2- or -CH=; the broken line ----- represents an optional double bond between R4 and R5; and R5 is a 5- or 6-membered substituted or unsubstituted unsaturated heterocyclic or heteroaromatic ring, or R5 is a substituted heterocyclic ring containing the substituent = O or = S, wherein the heteroatom is selected from S, O or P, and wherein R5 is optionally attached to R4 through a substituent on the heterocyclic or heteroaromatic ring; or a pharmaceutically acceptable prodrug, metabolite, ester, salt, derivative, tautomer or isomer thereof. The compounds have utility as COX-inhibitors and for use in the treatment of pain, inflammation or a neurodegenerative disease.
CN103520111A Florfenicol dry suspension, and preparation method and application thereof The invention provides a florfenicol dry suspension, which is composed of the following raw materials by weight: 8-12 parts of florfenicol, 7-9 parts of sodium citrate, 20-25 parts of mannitol, 0.5-1 part of milk essence, 48-55.5 parts of a sucrose powder and 6-8 parts of carboxymethyl cellulose or hydroxypropyl methyl cellulose. The florfenicol dry suspension prepared by the invention significantly improves the dispersion of florfenicol in water, increases the utilization rate of the drug, ensures good taste and improves animal compliance; at the same time, the dry suspension provided by the invention has good stability, is easy for product storage and transportation, and provides a new choice for veterinary medicine.
WO2010122927A1 Pharmaceutical agent for prevention or treatment of retarded nerve regeneration induced by diabetes Disclosed is a pharmaceutical agent for preventing or treating retarded nerve regeneration induced by diabetes. Specifically disclosed is a prophylactic or therapeutic agent for diabetic neuropathy, which comprises a compound represented by general formula (I) [wherein R1 represents a C1-C4 alkyl group; R2 and R3 independently represent a hydrogen atom or a C1-C4 alkyl group; R4 represents a hydrogen atom or a C1-C4 alkyl group; R5 represents a hydrogen atom, a C1-C4 alkyl group, a C2-C5 alkanoyloxymethyl or 1-(C2-C5 alkanoyloxy)ethyl group, a C1-C4 alkoxycarbonyloxymethyl or 1-(C1-C4 alkoxycarbonyloxy)ethyl group, a (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl group, a (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methyl group, or a phthalidyl group; and R6 represents a carboxy group or a tetrazol-5-yl group], or a pharmacologically acceptable salt or a pharmacologically acceptable ester thereof as an active ingredient.
CN101945659A Adrenomedullin production enhancer It is intended to find a substance having an action of effectively enhancing the production of adrenomedullin and to provide an adrenomedullin production enhancer using this substance. The adrenomedullin production enhancer is characterized by containing a ginsenoside, a sanshool and/or a shogaol as active ingredients.
CN101254205A Pd complex compound of carbohydrates derivative, preparing method thereof and applications of complex compound for curing cancer The invention relates to a palladium complex containing carbohydrate and a preparation method thereof, particularly to a palladium complex containing carbohydrate derivative and diamine ligand with anticancer effect, a pharmaceutical composition containing the same, and a preparation method thereof. The nitrogen ligand-containing palladium complex is prepared by reacting Alpha-D-mannopyranoside-3-diamine and a palladium complex at 0-80 DEG C.
US20100273773 Dibenzoazepine and dibenzooxazepine trpa1 agonists The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacological tools, or as irritant incapacitants, or in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.
WO2010150014A1 5r- 5 -deuterated glitazones for respiratory disease treatment A composition comprising a 5R-5-deuterated glitazone or a salt thereof, in which composition the 5R-5 deuterated glitazone component includes less than 5% by weight in total of 5R-5-protonated glitazone, 5S-5-protonated glitazone and 5S-5- deuterated glitazone. The glitazone may be rosiglitazone or pioglitazone. Compositions may be for pulmonary inhalation for treatment of Pulmonary inflammatory disease.
US20120190632 Anti-bacterial infection, inflammation, and leukemia composition and use thereof A method of inhibiting the growth of Gram-positive bacteria comprising administering an effective amount of Tellimagrandin II, its pharmaceutically acceptable salt, enantiomer, isomer or tautomer to a subject is provided. The Gram-positive bacteria comprise methicillin-resistant Staphylococcus aureus. A method of treating sepsis comprising administering an effective amount of Tellimagrandin II, its pharmaceutically acceptable salt, enantiomer, isomer or tautomer to a subject is also provided. A method of treating leukemia comprising administering an effective amount of Tellimagrandin II, its pharmaceutically acceptable salt, enantiomer, isomer or tautomer to a subject is further provided.
CN103263621A Medicine composition for treating lumbar diseases The invention discloses a medicine composition for treating lumbar diseases. The composition comprises the raw medicinal materials including antlers, rhizoma acori graminei, earthworm, vermilion, spina gleditsiae, camphor, rhizoma Homalomenae, drynaria rhizome, achyranthes aspera, elderberry, paris polyphylla, lycopodium clavatum, dendrobium nobile, groundsel, hematoxylon, radix et caulis ventilaginis leiocarpae, musk and the like. The medicine composition is prepared into clinically acceptable emplastrums, ointments, spray, liniments or tinctures by adding conventional auxiliary materials according to conventional processes. The medicine composition disclosed by the invention has the effects of promoting blood circulation to remove blood stasis, warming and activating meridian, enlightening and chilling the bone, has remarkable effects on treating lumbar diseases such as lumbar vertebra hyperostosis, lumbar disc herniation, lumbar muscle strain, rheumatism or rheumatoid lumbago, and is free of toxic and side effect.
CN103040775A Lenampicillin hydrochloride medicinal composition and preparation method thereof The invention relates to a lenampicillin hydrochloride medicinal composition and a preparation method thereof. The provided lenampicillin hydrochloride medicinal composition comprises 10 to 80 percent of medicinal active ingredient and 90 to 20 percent of pharmaceutically acceptable auxiliary materials. The composition is characterized in that the medicinal active ingredient is lenampicillin hydrochloride; and the pharmaceutically acceptable auxiliary materials comprise filling agent, disintegrating agent, adhesive and lubricating agent. The provided medicinal composition has an obvious treatment effect on respiratory tract, urinary tract and skin soft tissue infection and the like caused by sensitive bacteria; the medicament has good mouthfeel; and through a reasonable proportion, the cost of the medicament is reduced.
US20120076775 Combination of HGF Inhibitor and EGF Inhibitor to Treat Cancer The present invention is directed toward a method of treating cancer by administering to a patient an inhibitor of Hepatocyte Growth Factor and an inhibitor of, e.g., Epidermal Growth Factor.
WO2008045543A1 Substituted 4h-imidazo [4, 5, 1-ij] [1, 6] naphthyridine-9-amines and their pharmaceutical use Substituted 4H-imidazo[4,5, 1-ij][1,6]naphthyridine-9-amines of the Formula I : pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
WO2013090227A1 Benzisothiazol-3(1h)-one-5-sulfonyl derivatives as chemokine receptor modulators The present invention relates to novel benzisothiazol-3(1 H)-one-5-sulfonyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
CA2829187A1 Dipyridylamine derivative [Problem] To provide a compound having an excellent glucokinase-activating effect or a pharmacologically acceptable salt thereof. [Solution] A compound represented by general formula (I) or a pharmacologically acceptable salt thereof. In general formula (I): R1 represents a C6-10 aryl group, which may independently have one to five substituents selected from substituent group (A) or the like; X represents a single bond or the like; R2 represents a C6-10 aryl group, which may independently have one to five substituents selected from substituent group (A) or the like; R3 represents a 1H-tetrazol-5-yl group or a 5-oxo-4,5-dihydro-[1,2,4]oxadiazol-3-yl group; substituent group (A) is a group consisting of halogen atoms or the like; and substituent group (B) is a group consisting of halogen atoms or the like.
CN103417530A Method for applying artemisinin derivative and lipidosome of artemisinin derivative to preparation of sound sensitive agent The invention discloses a method for applying artemisinin derivative and lipidosome of the artemisinin derivative to preparation of a sound sensitive agent. When the artemisinin derivative and the lipidosome of the artemisinin derivative are used as the sound sensitive agent to prepare sound power drugs, the safety performance is high, and sound power antitumor activity is high.
CA2261040C Pharmaceutical composition comprising combination useful for treatment or prevention of arteriosclerosis or xanthoma A pharmaceutical composition comprising as its active ingredients one or more drugs selected from the group consisting of angiotensin II receptor antagonists and angiotensin converting enzyme inhibitors, and one or more insulin resistance improving agents exhibits excellent arteriosclerotic progress inhibitory effects, and is useful as a drug, particularly as a drug for the prevention or treatment of arteriosclerosis.
US20100247528 Arrays, kits and cancer characterization methods The invention provides an array comprising a substrate and a set of addressable elements, wherein each addressable element comprises (i) a polynucleotide that specifically binds to a target molecule, (ii) a polypeptide that specifically binds to target molecule, or (iii) a combination of (i) and (ii), wherein the target molecule is selected from the group of cancer-related target molecules as defined herein. Related kits, methods, and uses as described herein are further provided by the invention.
WO2011025167A3 Pharmaceutical composition for preventing or treating cancer comprising 2,6-substituted 3-nitropyridine derivative compound or pharmaceutically acceptable salt thereof Provided is a pharmaceutical composition for preventing or treating cancer comprising a 2,6-substituted 3-nitropyridine derivative compound or a pharmaceutically acceptable salt thereof. The pharmaceutical composition of the present invention can be used to advantage in treating cancer and preventing cancer as it effectively inhibits the growth of cancer cell lines and the activity of heat shock factor 1.
WO2014164617A1 Cosmetic use of napthoic acid derivatives Cosmetic compositions comprising napthoic acid derivatives and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The napthoic acid derivatives are believed to have modulatory activity against one or more biochemical pathways implicated in the appearance of human skin.
WO2008025073A1 Method of modulation of expression of epidermal growth factor receptor (egfr) involving mirna The present invention relates to a method for modulating the expression of epidermal growth factor receptor (EGFR) and its downstream signalling effectors. In particular, the present invention relates to a method for modulating the expression of epidermal growth factor receptor (EGFR) or like molecule in a cell comprising contacting said cell with an agent capable of directly or indirectly interacting with the 3 ' -untranslated region (UTR) of the mRNA of said EGFR or like molecule, wherein the UTR is encoded by a sequence which comprises a sequence having at least about 70% identity with at least one sequence selected from the group consisting of the sequences set forth in SEQ ID NOs: 1-36.
WO2008018447A1 Aminoalcohol derivative and immunosuppressant containing the same as active ingredient Disclosed is an aminoalcohol derivative which is useful as an excellent immunosuppressant. Specifically disclosed is an aminoalcohol derivative represented by the general formula (1) below, which is a highly safe compound having excellent immune suppressing activity.
US20060088820 Detecting superantigen activity in a biological sample Multiple sclerosis or a condition associated with multiple sclerosis is detected by detecting an amount of lymphocytes bearing a Vβ16, Vβ17 or Vβ7 determinant and calculating an amount of expansion or loss of these lymphocytes.
CN101538304A Fungi mixture and method for preparing same The invention provides antrodia cinnamomea compound components and antrodia cinnamomea composition components, and additionally provides a fungi mixture and a method for preparing the same. Particularly, the invention relates to a method for producing fungi in a large quantity with a colloid culture medium.
US7105528 exhibit a surprising strong efficacy in lowering the intraocular pressure; excellent duration of action; excellent tolerability The invention provides a compound of formula I wherein A, B, X, Y and R1 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.
CN101007048A Preparation method of a compound glutamine medicine composition The invention relates to a process for preparing compound pharmaceutical composition of glutamine, which is a mucosa preservative for digestive tracts prepared from raw materials of L-glutamine, ginseng, licorice root, white atractylodes rhizome and poria cocos wolf.
US20120177634 Demethylpenclomedine analogs and their use as anti-cancer agents This disclosure concerns novel demethylpenclomedine analogs. Also disclosed are pharmaceutical compositions and methods for using such compositions to treat hyperproliferative disorders. In one embodiment the analogs are represented by the formula
CN103285411A Preparation method of poly(lactic-co-glycolic acid based magnetic medicine-carrying hollow microspheres The invention relates to a preparation method of poly(lactic-co-glycolic acid based magnetic medicine-carrying hollow microspheres. The preparation method comprises the following steps: adding magnetic Fe3O4 nanoparticles into a poly(lactic-co-glycolic acid solution so as to obtain an oil phase, dissolving a hydrochloric acid doxorubicin DOX into ultrapure water so as to obtain a water phase, mixing the oil phase with the water phase, and carrying out ultrasonic processing so as to obtain a W/O (water-in-oil) emulsion; adding the W/O emulsion into a polyvinyl alcohol PVA solution, and homogenizing so as to obtain a W/O/W (water-oil-water) emulsion; adding the W/O/W emulsion into an isopropyl alcohol aqueous solution, stirring for 1-4h, carrying out centrifugal washing, dispersing the obtained mixture in water, and finally carrying out freeze drying. According to the preparation method, the preparation process is simple, and experiment conditions are normal pressure and temperature; and the product prepared according to the preparation method has a good US/MRI imaging effect and a good medicine sustained release effect, and provides a reference for the development of novel multi-functional therapeutic and diagnostic medicaments.
US20080234287 Lung cancer, gastric cancer, liver cancer, leucocythemia, endometrioma, oophoroma, mammary cancer, colon cancer, prostatic cancer, or pituitary gland cancer; N (N',N'-dimethylaminoethyl)benzo[b]thieno[2,1-c]naphthalimide The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5- or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities to the proliferation of various tumor cells such as human lung cancer, gastric cancer, liver cancer, leucocythemia and the like. The inhibition of cell proliferation is dose-dependent.
US20130022686 Combinations of liquid filtration media and methods for enhanced filtration of selected water contaminants By sequentially aligning various filtration media and delivery systems, enhanced synergistic reduction of water contaminants is obtained compared to the prior art or separate use of the individual media/filters. Specific filtration media are formulated with proper proportioning and sequencing to enhance the ability to reduce metals that cause staining, odors and bad taste such as iron, copper and manganese. Also disclosed is the reduction of potentially hazardous metal radionuclides metals such as uranium, iodine, cesium, plutonium and radium. Also disclosed is improved removal of heavy metals such as arsenic, lead, chromium, and mercury as well as organic compounds such as halogenated carcinogenic compounds. The present devices and methods remove specific bacteria and their toxins from water to reduce the risk of dermatitis. Thus, the present invention enhances our ability to achieving cleaner and safer water for drinking, swimming, washing, bathing and cooking.
US20110160270 Deuterium-enriched sdx-101 The present application describes deuterium-enriched SDX-101, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
EP1868437A1 Method of treating or preventing bone deterioration or osteoporosis The present invention relates to a transdermal hydroalcoholic testosterone gel formulation and a method for treating, preventing, or reducing the risk of developing deterioration of bone. The present invention also relates to a method for treating, preventing, or reducing the risk of developing osteoporosis.
EP0715856B1 Keratin-storable antifungal composition for external use A keratin-storable antifungal composition for external use, which contains an antifungal with a high keratin affinity as the active ingredient and also contains at least one liquid oily substance selected from among methyl salicylate, glycol salicylate, crotamiton, mentha oil and methol, and wherein the antifungal has an enhnaced capability of penetrating into kerating and is improved in the restorability therein.
US20120052012 Highly biocompatible dual thermogelling chitosan/glucosamine salt compositions The present disclosure relates to a chitosan solution neutralized with amino-sugar carbonate buffering solution or amino-sugar phosphate buffering solution or phosphorylated aminosugar buffering solution. The resulting thermogelling chitosan composition is highly biocompatible, isotonic and has the ability to rapidly turn into gel upon heating to the body temperature. It provides a novel chitosan-based composition to suitable for drug delivery, cell delivery and repair or regeneration of tissues and organs as well as other clinical treatment.
CN103393689A Pharmaceutical composition of cefotiam hydrochloride for injection and compound amino acid injection The invention relates to a pharmaceutical composition of cefotiam hydrochloride for injection and compound amino acid injection, and especially relates to an application product of the pharmaceutical composition, wherein the application product comprises cefotiam hydrochloride for injection and compound amino acid injection. Administration method comprises following steps, 0.25 to 2g of cefotiam hydrochloride for injection is dissolved in appropriate amount of compound amino acid injection, and the mixture is applied to 30min to 2h of intravenous drop infusion, wherein 0.25 to 2g of cefotiam hydrochloride is the dosage of one time. Compared with a method of compatible mixing application of cefotiam hydrochloride for injection and compound amino acid injection, the pharmaceutical composition is capable of simplifying steps, improving safety, and increasing clinical application quality and bioavailability of medicines, and possesses significant benefits on the stability of cefotiam hydrochloride.
US20110059910 Novel aromatic fluoroglycoside derivatives, pharmaceuticals comprising said compounds and the use thereof The invention relates to substituted aromatic fluoroglycoside derivatives, and to the physiologically compatible salts and physiologically functional derivatives thereof. The invention also relates to methods of lowering blood sugar and the treatment of type I and type II diabetes.
US20110262496 Therapeutic formulation for reduced drug side effects The present invention provides drug therapy formulations for reducing the side effects associated with a therapeutic. In some embodiments, the present invention provides a reduction in sleep- and diet-related side effects associated with a therapeutic.
EP1769799A2 Pharmaceutical compositions containing steroidal structures and uses thereof There is provided a pharmaceutical composition comprising (i) a compound of the formula wherein: X is a hydrocarbyl ring having at least 4 atoms in the ring; K is a hydrocarbyl group; Rs is a sulphamate group; (ii) optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant, wherein the compound is present in an amount to provide a dosage of no greater than 200 µg/day.
US7919116 Controlled release metformin formulations Sustained release pharmaceutical formulations comprising an antihyperglycemic drug or a pharmaceutically acceptable salt thereof are disclosed. The formulations provide therapeutic plasma levels of the antihyperglycemic drug to a human patient over a 24 hour period after administration.
US20080182870 PYRIDO(3,2-d)PYRIMIDINES USEFUL FOR TREATING VIRAL INFECTIONS Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I): wherein: R4 is hydrogen, and R1, R2 and R3 together provide a specific substitution pattern, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, are useful in the treatment of hepatitis C.
CN101084888A Tea pigment lozenge The invention discloses a health lozenge which comprises the following constituents (by weight percent): tea pigments 20-35%, crystal sugar 30-45%, starch 20-35% and peppermint oil 0.5-1.5%.
WO2014089004A1 Methods for treating 5-fluorouracil prodrug non-responsive cancer patients Methods for treating a patient who had rapid disease progression on a 5-FU prodrug regimen comprising first administering to the patient a DPD inhibitor that substantially eliminates activity of the enzyme in both nervous and non-nervous tissues within the patient and thereafter administering 5-FU, wherein the level of 5- FU is in substantial excess of DPD inhibitor in the patient are envisioned. Also encompassed herein are a DPD inhibitor for use in a combined treatment with 5-FU, a combination for treating a patient having rapid disease progression on a 5-FU prodrug regimen comprising a DPD inhibitor and 5-FU, and use of eniluracil in combination with 5-FU for the manufacture of a medicament for treating a patient having rapid disease progression on a 5-FU prodrug regimen.
WO2010151074A3 Photosensitizer containing conjugates of quantum dot-chlorine derivatives and composition for treating and diagnosing cancer containing same for photodynamic therapy The present invention relates to a photosensitizer containing conjugates of quantum dot-chlorine derivatives and a composition for treating and diagnosing cancer containing the same for photodynamic therapy. The conjugates of the present invention can be used as a single medicine for treating and diagnosing cancer.
US20080292591 localized foci of model tumor cells highly correlated to actual clinical tumor cells; genetic engineering; drug screening This invention provides model systems for study of tumors. Model cells and model animals are prepared to mimic characteristics of natural clinical tumors. The tumor models can be contacted with putative modulators to screen for therapeutics and to help understand tumorigenic processes. Model animals can include model cells, closely correlated to the characteristics of clinical tumors, in an environment closely mimicking that of the tumors in patients. Thus, the animal models are highly representative for use in clinical and pharmacological studies.
EP1999121A1 Novel tetralins as 5-ht6 modulators The present invention relates to new compounds of formula I, or salts, solvates or solvated salts thereof, wherein Q, R1, R2, R3, R4 and n are defined as in claim 1, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
US20100216749 Combination Therapy for Neuroprotection The present invention relates to combination therapy of a pyruvoyl derivative and an anti-oxidant, which is characterized by significant increase of the activity of microglia, inhibition of brain tissue damage by the activation of inflammatory cytokines, improvement of motor skill and recovery effect of neuronal damage. Compared to single treatment with each, this present invention provides a continuous high neuroprotective effect even after 6 hours from the onset of damage.
CA2607419A1 Granular preparation containing biguanide compound A granular preparation comprising a biguanide compound and a solidification-preventive agent which does not solidify during storage and therefore can eliminate a difficulty to take the preparation.
CN103694377A Amphiphilic C-6-(4-(methyl amino)-1,2,3-triazole)deoxidized inulin derivatives and preparation and application thereof The invention relates to amphiphilic C-6-(4-(methyl amino)-1,2,3-triazole)deoxidized inulin derivatives and a preparation and an application thereof. The amphiphilic C-6-(4-(methyl amino)-1,2,3-triazole)deoxidized inulin derivatives are as shown in formula (1), wherein n has an average range of 10-35. The preparation method comprises the following steps: halogenating the primary hydroxyl group of raw material inulin, performing acyl protection of hydroxy groups at the other sites, allowing the inulin to react with sodium azide or lithium azide at 40-70 DEG C for 8-24 hours, performing purification to obtain 6-azido-3,4-diacyl-6-deoxidized inulin, allowing the 6-azido-3,4-diacyl-6-deoxidized inulin to react with propynylamine through a click chemistry reaction to obtain the amphiphilic C-6-(4-(methyl amino)-1,2,3-triazole)deoxidized inulin derivatives. The mole amount of the sodium azide or lithium azide is 1-2 times as many as the that of the raw material inulin; the mole ratio of the propynylamine to the raw material inulin is 2-3:1. The product of the invention is wide in application, simple in synthetic steps, easy to popularize, and easily available in required equipment and raw materials.
CN103626776A Pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives, preparation methods of pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives, and application of pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives in oncotherapy The invention relates to pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives or medical salts thereof, as well as application of the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives or the medical salts thereof. The pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives and the medical salts thereof have the structure shown as the formula I. Pharmacological experiments show that the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives and the medical salts thereof have inhibiting effects on the proliferation of various tumor cells. Moreover, the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives are small in toxicity, have the advantages of selectivity on tumor cells, and are dual-functional anti-tumor drugs. Meanwhile, the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives are easy to synthesize, and the overall yields are high. All the advantages show that the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives have great potential of being anti-tumor drugs.
EP2180889A1 Extracts with liver-x-receptor modulators, compounds and their use especially in weight control The invention relates to the use, or methods (especially with regard to animals, especially human, that are in need of such treatment) comprising the use, of an extract and/or one or more natural compounds from plants or parts of plants, respectively, from a genus selected from the group consisting of Schisandra, Illicium, Kadsura, Steganotaenia and Magnolia, alone or as supplement, as active ingredient in the regulation of body weight and/or fat loss and/or for the management of obesity, either in humans or in animals, to the use of said extract and/or natural compound(s) or mixtures in the manufacture of a pharmaceutical or nutraceutical formulation for the regulation of body weight and/or fat loss and/or for the management of obesity either in humans or in animals. The above extract and/or compound(s) can further be used to reduce one or more adverse metabolic parameters in a subject. The invention relates also to said extract and/or compound(s) for use in the treatment or in the preparation of a medicament for the treatment of obesity, as well as their preparation. It also relates to pharmaceutical or nutraceutical formulations comprising said extract and/or natural compound(s) which are useful in the regulation of body weight and/or fat loss and/or for the management of obesity.
WO2006069466A1 Series of triterpenoid ptp1b inhibitors and their preparing method and use The invention discloses series of triterpenoid PTP1B inhibitors of following formula (I), and the pharmacologic studies further suggests such compounds or their physiological acceptable salts have the activity of inhibiting PTP1B, thus these compounds can be the euglycemic agents and can be used to prepare the medicament for the treatment of the disorders caused by insulin resistance. The invention also relates to a process for preparing such compounds.
CN101007012B An oral mucosal absorbent preparation containing active components of astragaloside IV The invention relates to an oral mucosa absorption agent containing active astragaloside constituent and the process for preparation, wherein the weight proportions of each constituents include active constituent of astragaloside 0.2-20%, dispersing agent 0-60%, bonding agent 0.5-5.0%, lubricating agent 0.5-5.0%, filling agent 10-95%, transdermal absorption promoting agent 0-10%. The agent is capable of improving medicament dissolution property and accelerating dissolving out speed.
US20130023488 Methods and compounds for reducing intracellular lipid storage Compounds and compositions for reducing intracellular lipid accumulation in a cell are described herein. These compounds are useful for the treatment and prevention of lipid/glycogen disorders, as well as for the treatment and prevention of obesity. A high throughput screen for identifying compounds that reduce intracellular lipid accumulation in cells is also provided.
CN101161288A Enganced tumour cell cracking article of oligonucleotide and method for treating knub Tumor cell lysates reinforced by oligonucleotides and method for treating tumor by using with the same are provided in the present invention. The tumor cell lysates are various cell lysates. The source of tumor cells can be from autogenous tumor, allograft tumor cell and various tumor cell lines cell. The oligonucleotides comprises but not only CpG containing oligonucleotides. Tumor cell lysates reinforced by oligonucleotides has curative effect to corresponding tumor applyied to individual.
US20070041866 Aqueous solution of olanexidine, method of preparing the aqueous solution, and disinfectant The present invention provides a disinfectant that contains olanexidine in a concentration sufficient to exhibit an effective bactericidal effect, and that has hardly any side effects such as skin irritation. Specifically, the present invention provides a disinfectant containing an aqueous solution that contains olanexidine and at least an equimolar amount of gluconic acid, and substantially contains neither an acid other than gluconic acid nor a salt of the acid other than gluconic acid.
CN101486688B DPP-IV inhibitor with sulfonyl amine acyl alkyl piperazine structure The invention pertains to the field of medical technology, particularly relating to a DPP-IV inhibitor with a sulfonyl-amide alkyl piperazine structure, which is shown in the general formula (I), and pharmaceutically acceptable salt or an isomer thereof, wherein, Ar, Ar', R<1> and n are defined as the instruction book; the invention also relates to a preparation method of the compounds, a pharmaceutical composition containing the compounds and applications of the compounds in the preparation of medicaments for treatment and/or prevention of diabetes, noninsulin-dependent diabetes, hyperglycemia, insulin resistance.
CA2477474C Cyclic n-substituted alpha imino carboxylic acids for selective inhibition of collagenase The invention relates to compounds of formula (I), which are suitable for the production of medicaments for the prophylaxis and therapy of diseases in the course of which reinforced activity of matrix metalloproteinase 13 is involved. Said diseases include degenerative arthropathy, for example, spondylosis, chondroporosis after joint trauma or prolonged joint immobilization after meniscus or patella injuries or ruptures of a ligament or a disease of the connective tissue such as collagenosis, periodontal diseases, wound healing disorders or a chronic disease of the locomotor system such as acute or chronic inflammatory, immunological or metabolic arthritis, arthropathy, myalgia or bone metabolism disorders or an ulceration, arteriosclerosis or stenosis or an inflammatory disease or a cancer disease, tumor metastasis formation, cachexia, anorexia or septic shock.
CN101092414A Preparation and application of a category of 6 ¿C aryl ¿C 3 ¿C cycroamido methyl pyrone derviation This invention relates to compounds with 6-aryl-3-cycloaminomethyl pyrone structure, their preparation method and their application. Pharmacological activity experiments show that the compounds have a high activity in selectively inhibiting AChE while no obvious activity in inhibiting BuChE. The activity of the compounds in inhibiting AChE is higher than huperzine A. Mouse in vivo tests show that the compounds do not have acute toxicity or abnormal reaction phenomenon, and the compounds can be used as a kind of new drugs for treating Alzheimer's disease.
CN103006791A Toothache stop tablet and preparation method thereof The invention discloses a toothache stop tablet and a preparation method thereof. The preparation method comprises the following step of: (1) weighing long pepper, clove and borneol; (2) adding long pepper in an ethanol water solution to reflux and extract, filtering, recycling ethanol until a dense extract, of which the relative density is 1.1-1.3 when the temperature is 70-90 DEG C, is obtained, adding the ethanol water solution, uniformly mixing, standing, taking supernatant liquor, reducing pressure, and concentrating to obtain a first extract; (3) extracting clove oil from clove through steam distillation to obtain a second extract; and (4) mixing the first extract, the second extract and clove to obtain a mixture, adding an lubricating agent and a thinning agent, uniformly mixing, and tabletting to obtain the toothache stop tablet. The tablet prepared by the method is quick in effect, convenient to take and obvious in treatment effect, and can treat both symptoms and root, thereby being capable of meeting requirements of a great number of patients.
US8409578 Methods for treating bone loss with antibodies to OPGL Antibodies that interact with osteoprotegerin ligand (OPGL) are described. Methods of treating osteopenic disorders by administering a pharmaceutically effective amount of antibodies to OPGL are described. Methods of detecting the amount of OPGL in a sample using antibodies to OPGL are described.
WO2011070781A1 Substituted aminothiazine derivative Disclosed is a a therapeutic or prophylactic agent for diseases induced by the production, secretion and/or deposition of amyloid-β protein. Specifically disclosed is a compound represented by formula (I) (wherein R1, R2a, R2b, R3, R4a, R4b, ring A and the dotted line are as defined in the description), a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt.
US20120302518 Polymorphic Form Of N-(S)-(3,4-Difluoro-2-(2-Fluoro-4-Iodophenylamino)-6-Methoxyphenyl)-1-(2,3-Dihydroxypropyl)Cyclopropane-1-Sulfonamide And Uses Thereof Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
US20080027071 2-{2-[4-(2,3-Dihydrobenzo[1,4]dioxin-5-yl)piperazin-1-yl]ethylsulfanyl}-6-methylnicotinonitrile; serotonin and dopamine receptor antagonist, serotonin reuptake inhibitor; anxiolytic agent, antidepressant; panic and obsessive compulsive disorder, social phobia, eating disorders, psychosis A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disorders, and neurological disorders such as psychosis.
CN103181906A Itraconazole flavoured tablet for pets and preparation method for the same The invention discloses an itraconazole flavoured tablet for pets and a preparation method for the same. The itraconazole flavoured tablet disclosed by the invention is rapid to release medicine and safe in medication. The itraconazole flavoured tablet is composed of itraconazole, a disintegrant, a filler, an adhesive, a lubricant and a flavouring agent. The itraconazole flavoured tablet prepared by the preparation method disclosed by the invention has the characteristics of being convenient to administrate, rapid to act, high in blood concentration, and stable in curative effect.
CN102085194A Levetiracetam oral disintegrating tablet and preparation method thereof The invention provides a levetiracetam oral disintegrating tablet and a preparation method thereof. The levetiracetam oral disintegrating tablet is prepared by adopting a freeze drying process and contains levetiracetam as an active constituent, polyethylene glycol 6000 as a solid dispersing agent, maltodextrin as a freeze-drying protective agent and hydrolyzed gelatin as an adhesive. The levetiracetam is a novel antiepileptic drug, and the levetiracetam oral disintegrating tablet provided by the invention has the advantage of improving the medication compliance of patients and the curative effect.
WO2011143755A1 Compositions and methods of treating schizophrenia There is described herein compositions and methods for the treatment of schizophrenia in a patient. The compositions comprise a NO donor and the methods involve the administration of a NO donor to a patient.
CN101940588A Application of benzoylated phaeophyceae polysaccharide for preparing medicines for treating Parkinson disease The invention relates to application of benzoylated phaeophyceae polysaccharide for preparing medicines for treating Parkinson disease, which is characterized in that 1mg/ml of the benzoylated phaeophyceae polysaccharide has the action on protecting nerves and can resist the cell damage induced by neurotoxin 6-hydroxy dopamine and high ferrum and reduce the generation of reactive oxygen substances in the cells induced by the neurotoxin 6-hydroxy dopamine and high ferrum; the benzoylated phaeophyceae polysaccharide is prepared from natural phaeophyceae polysaccharide by benzoylation; the natural phaeophyceae polysaccharide comes from other phaeophyceaes of kelp seaweeds or gulfweeds, sea mustards, sargassum fusiforme, sargassum thunbergii kuntze, sargassum kjellmanianum, kelp, and the like; the phaeophyceae polysaccharide has the advantages of rich sources and high safety; and the phaeophyceae polysaccharide has the protection action on the cell damage induced by neurotoxin and high ferrum. The invention has an important application value on developing a novel I-class natural medicine for treating Parkinson disease in China.
CN101385727A Thiazone and inorganic acid composition for treating malignant entity tumor, preparation method and uses thereof The invention relates to a composition of a clinically applied transdermal penetrant thiazone, one or more of common inorganic acids, such as hydrochloric acid, sulfuric acid, nitric acid and phosphoric acid and water, a preparation method and a method thereof, in particular to an application in the aspect of treating malignant solid tumors.
EP1372648B1 Tie2 receptor kinase inhibitors for treating angiogenic diseases The present invention relates to novel compounds and the treatment of mammalian diseases in which inappropriate, excessive or undesirable angiogenesis has occurred and/or where excessive Tie2 receptor activity has occurred.
US7320982 Use of 4-substituted tetrahydropyridines for the manufacture of medicaments acting upon TGF-β 1 The invention relates to the use of a compound of formula (I): for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-β1.
US20100261795 Antiacneic compositions The invention relates to novel powerful and non-irritating formulations of antiacneic substances and polyolprepolymers. The invention further relates to novel formulations of polyolprepolymers in combination with, for example, benzoyl peroxide exhibit progressive release of the active with a decrease in irritating effects. These formulations may be therapeutically beneficial over existing acne therapies.
US7402606 Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.
WO2008060248A1 Indole sustituted pyrimidines and use thereof in the treatment of cancer The present invention relates to pyrimidine compounds of formula (I) that are useful as anti proliferative agents. More particularly, the present invention relates to indole substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers.
US20080081036 Using topical mixture to repair and condition animal skin Animal shampoo compositions and methods of using the same for topical treatment of pets in need of improvement of quality of skin are provided. Methods for preparing such shampoos are also provided.
CN101161668A Application of flavone c-glycosides in preparation of drugs curing and preventing hepatitis The present invention belongs to pharmacy field, and relates to the application of 5,7,4'-trihydroxy-glycosylflavones with the general formula belwo to preparation of drugs and health-care food used to prevent or treat HBV hepatitis, immunity hepatitis and alcoholic hepatitis, in which the R 1 represents glucose or arabinose, and R2 represents glucose or arabinose.
CA2587791C Method for treating neuropathic pain and associated syndromes The present invention is directed to the use of ibudilast for treating neuropathic pain.
CN102008501A Externally applied pharmaceutical composition as well as use method and application thereof The invention provides an externally applied pharmaceutical composition as well as a use method and an application thereof. The externally applied pharmaceutical composition comprises the following raw materials in parts by weight: 1-10 parts of rivanol and 900-1100 parts of calamine powder, preferably comprising 3-4 parts of rivanol and 990-1010 parts of calamine powder. In addition, pure cream, vanishing cream or vaseline can be added in the raw materials to be blended into paste. The externally applied pharmaceutical composition can be used for curing skin problems such as viral infection skin diseases, coccus infection skin diseases, allergic skin diseases, bullous dermatosis, skin abrasions of different areas, burns and scalds at the first degree and the second degree or decubitus and the like, is simple and convenient in use, is economical and practical, has rapid curative effect and high recovery rate up to 100%, has no irritation on wounded parts, causes no pains for patients after being applied on the wounded parts, and has no adverse effect.
US20100016254 Gemcitabine prodrugs, pharmaceutical compositions and uses thereof The present invention provides gemcitabine prodrugs, methods of making gemcitabine prodrugs, pharmaceutical compositions of gemcitabine prodrugs and methods of using gemcitabine prodrugs and pharmaceutical compositions of using gemcitabine prodrugs to treat or prevent diseases or disorders such as cancer or viral infections.
US20110195979 Compounds for the treatment and prevention of influenza A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.
CN103172633A Compound, and preparation method and application thereof The invention provides a compound disclosed as Formula I or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The new compound provided by the invention can effectively inhibit dipeptidyl peptidase-IV (DPP-IV) activity with better effects than the existing DPP-IV enzyme inhibitor Linagliptin; and meanwhile, the compound has the advantages of higher selectivity for DPP-IV, higher safety and lower toxic or side effect on the DPP inhibitor, and thus, provides a new medicine option for treating or/and preventing diseases related to DPP-IV enzyme activity.
US20100222430 Method of Treating Post-Surgical Acute Pain A method is provided for treating pain in patients recovering from post-surgical trauma by administering between about 13 to about 30 mg of diclofenac potassium in a liquid dispersible formulation over a period of at least 24 hours, wherein the daily total amount of diclofenac potassium administered is less than or equal to about 100 mg. The method is particularly useful in treating acute pain in bunionectomy patients.
CA2851619A1 The use of (2r, 6r)-hydroxynorketamine, (s)-dehydronorketamine and other stereoisomeric dehydro and hydroxylated metabolites of (r,s)- ketamine in the treatment of depression and neuropathic pain The disclosure provides pharmaceutical preparations containing (2R,6R)-hydroxynorketamine, or (R)- or (S)-dehydronorketamine, or other stereoisomeric dehydro or hydroxylated ketamine metabolite. (2R,6R)-hydroxynorketamine The disclosure also provides novel ketamine metabolite prodrugs. The disclosure provides methods of treating, bipolar depression, major depressive disorder, neuropathic and chronic pain, including complex regional pain disorder (CRPS) by administering a purified ketamine metabolite or a ketamine metabolite prodrug directly to patients in need of such treatment.
US20110245273 Novel aliphatically substituted pyrazolopyridines, and the use thereof The present application relates to novel aliphatically substituted pyrazolopyridines, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.
US8389551 Optical enantiomers of phenyramidol and process for chiral synthesis The present invention discloses optically pure (R) and (S) Phenyramidol enantiomers and their pharmaceutically acceptable salts, a process for synthesizing such enantiomers by means of a styrene oxide based synthesis, and also a clinical evaluation of (R) and (S) enantiomers of Phenyramidol, their salts and compositions thereof for enhanced/newer therapeutic benefits.
WO2014058736A1 Neuroactive 19-alkoxy-17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same The present disclosure is generally directed to neuroactive 19-alkoxy-17(20)-Z-vinylcyano-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
CN101313890A N,N-di-alkyl aminophenol ester salt injection of 2,6-di-isopropyl phynol The invention relates to a pro-drug of 2,6-diisopropylphenol, namely an injection of 2,6-diisopropylphenol N, N-dialkyl amino-acid ester salts, comprising the following compositions: 2 to 200g of 2,6-diisopropylphenol N, N-dialkyl amino-acid ester salts (counted by the 2,6-diisopropylphenola), 0 to 4g of additives for retarding oxidation, 10 to 100g of osmoregulator, 0 to 200g of excipient and 2,000 ml of water for injection. The 2,6-diisopropylphenol N, N-dialkyl amino-acid ester salts have good water-solubility, can produce the 2,6-diisopropylphenol quickly in human body, can be made into injections in the forms of water needle, transfusion, frozen powder injection agent, sterile separation packed powder injection and sterile liquid storage to eliminate side effects possibly produced by 2,6-diisopropylphenol emulsion, thereby the production and use are highly safe, and prepared various injections improve the safety and effectiveness of medicating. The preparation process is simple and safe, and the product quality is easy to control.
CN101711862A Medicine target spot relevant to inflammatory diseases and application thereof The invention relates to a medicine target spot relevant to inflammatory diseases mediated by immunological cells and an application thereof. The medicine target spot is gamma-aminobutyric acid transport protein subtype 1 (GAT-1). The invention discloses GAT-1 or an application of an agonist thereof used for preparing a composition suppressing the inflammatory diseases mediated by the immunological cells of mammals. The invention also discloses a method for sieving a potential substance suppressing the inflammatory diseases mediated by the immunological cells of the mammals.
US6972289 dehydrodiketopiperazines such as dehydrophenylahistin used as antitumor agents; dipeptides The present invention relates to a cell division inhibitor comprising various dehydrodiketopiperazines such as dehydrophenylahistin, or analogs thereof as an active ingredient, and a dehydrogenase and a method for producing the same inhibitor.
EP2440250A1 Targeted liposomes comprising n-containing bisphosphonates and uses thereof The present is based on the finding that folate targeted liposomal alendronate (FT-AL-L) was significantly more potent against two tested cancer cell lines than the free alendronate (AL) or the non-targeted liposomal alendronate (AL-L), as observed by the increased cytotoxicity of the folate targeted liposomal alendronate. Thus, the present disclosure provides targeted liposomes comprising a membrane and an intraliposomal core, the membrane comprising at least one liposome forming lipid and a targeting moiety, such as folate, exposed at the membrane's outer surface; and the intraliposomal core comprising encapsulated therein least one N-containing bisphosphonate. Also provided by the present disclosure are methods of use of the targeted liposomes such as for the treatment of a disease or disorder.
EP1928405A1 Pharmaceutical compositions for the treatment of inner ear disorders The present invention provides compositions containing (i) a pharmaceutically active agent selected from a group consisting of an arylcycloalkyamine or a derivative, analogue or pharmaceutically active salt thereof, and (ii) a biocompatible polymer or a combination of biocompatible polymers. These compositions or medicaments containing these compositions may be used for the prevention and/or treatment of inner ear diseases, e.g. tinnitus.
US20100137287 Aryl-and heteroaryl-substituted tetrahydrobenzo-1,4-diazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin The aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepine derivative compounds of the present invention are represented by formulae 1(A-D) having the following structure: where the substituents X and R1-R8 are as defined herein.
WO2010095926A1 Use of reveratrol for preserving cognitive functioning The present invention relates to the use of an hydroxylated stilbene, in particular resveratrol, in the manufacture of a neutraceutical composition for the treatment of age- and condition-related decline in brain neuronal function and/or cognitive functioning in a mammal. In particular, the condition is selected from the group of Alzheimer's Disease, dementia, depression, sleep disorders, impaired memory function, psychoses, Parkinson's disease, Huntington's chorea, epilepsy, schizophrenia, paranoia, ADHD and anxiety.
WO2008049644A1 Thymidine analogs for imaging The present invention relates to nucleoside analogues and more particularly to labeled nucleoside analogues. It has been found new thymidine analogues can be stably labeled with a detectable label moiety. Further the present invention relates to methods of making above compounds and use of such compounds for diagnostic imaging of tumor cells and / or treatment of proliferative diseases. In addition, the present invention relates to the preparation and use of positron emitting compounds for positron emission tomography (PET). A kit is also disclosed.
WO2009001562A1 Compositions and methods of treating cancer The invention features a method for treating cancer by administering a double-stranded nucleic acid molecule against a CX gene selected from the group consisting of C14orf78, MYBL2, UBE2S and UBE2T. The invention also features products, including the double-stranded nucleic acid molecules and vectors encoding them, as well as compositions comprising the molecules or vectors, useful in the provided methods. The methods of the invention are suited for the treatment of cancers including lung cancer, breast cancer, bladder cancer, esophagus cancer, prostate cancer, cholangiocellular carcinoma and testicular seminoma.
CN102743346A Small-size fat-soluble vitamin freeze-dried powder injection and preparation method and preparation device thereof The invention belongs to the technical field of freeze-dried powder injection preparation, and relates to a small-size fat-soluble vitamin freeze-dried powder injection, a preparation method and a production device thereof. The small-size fat-soluble vitamin freeze-dried powder injection is filled in a 7-ml tubular penicillin bottle; the product specification of the fat-soluble vitamin freeze-dried powder injection is fat-soluble vitamin I or II; the preparation method comprises the following steps: adding VA, VD2, VE, VK1, and a solvent into a container, stirring till dissolving to obtain a B solution; adding injection water into a preparation tank, cooling, weighing a vehicle, adding the vehicle for dissolution to obtain an A solution; adding the B solution into the A solution, uniformly stirring; weighing active carbon, adding the active carbon to perform adsorption for 30 min, performing filtration, fine filtration, filling the solution into a 7-ml tubular penicillin bottle, performing freeze-drying, tamping, and cover rolling to obtain the product. According to the invention, the package size is reduced; thus the yield is effectively increased; the package cost and the transport cost are reduced; and the freeze-drying and evaporation energy consumption is greatly reduced.
WO2012072033A1 Substituted 2,3-phthalazinone compounds and use thereof Provided are substituted 2,3-phthalazinone compounds, their isomers, salts, solvates, prodrugs, their preparation and the use for the preparation of medicaments for inhibiting the activity of poly (adenosine diphosphate-ribose) polymerase and the related diseases thereof.
US20080312417 Ucp5 The present invention is directed to novel polypeptides having homology to certain human uncoupling proteins (“UCPs”) and to nucleic acid molecules encoding those polypeptides. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention, and methods for producing the polypeptides of the present invention.
US20120196892 Novel caspase-2 inhibitors Novel compounds of formula (I) and slats thereof and pharmaceutical compositions which contain such a compound or salt are useful for inhibiting pro-apoptotic caspase-2 and for preventing and/or treating diseases and injuries where caspase-2 activity is implicated, in particular neonatal brain ischemia.
WO2006064757A1 Aminocarboxylic acid derivative and medicinal use thereof A compound represented by the general formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug of any of these; and a drug containing any of these. (I) (In the formula, all the symbols are as defined in the description.) The compound represented by the general formula (I) has the ability to combine with an S1P receptor (especially EDG-1, EDG-6, and/or EDG-8). It is useful for the prevention and/or treatment of rejection reactions to transplantation, graft versus host diseases, autoimmune diseases, allergic diseases, neurodegenerative diseases, etc.
WO2011135563A1 Metal entrapped bioactive composites The present invention provides composites comprising at least one bioactive agent entrapped within a matrix of at least one metal; wherein said composite controllably releases at least one of said bioactive agent and metal or ion thereof, processes for the preparation of composites of the invention, compositions and products comprising composites of the invention and various uses thereof.
WO2014142645A1 Antiviral activity of quercetin against japanese encephalitis virus The present invention provides an antiviral medicament for treating Japanese Encephalitis Virus (JEV) infection comprises a natural flavonoid compound namely quercetin. In the present invention, antiviral activity of quercetin was evaluated against JEV replication in African green monkey kidney cell line (Vero). Anti-JEV activities of quercetin were examined at different stages of JEV replication cycle. The effects of quercetin on virus replication were determined from Foci Forming Unit Reduction Assay (FFURA) and quantitative RT-PCR.
WO2011012897A1 New combinations for the treatment of asthma The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is (R)-7-(2-(2-fluoro-5-((4-(2-isopropylthiazole-4-carbonyl)-1-oxa-4,9-diazaspiro[5.5]undecan-9-yl)methyl)phenethylamino)-1-hydroxyethyl)-4- hydroxybenzo[d]thiazol-2(3H)-one or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase activator; an IKK2 kinase inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a PDE4 inhibitor; a PPARγ agonist; a protease inhibitor; a p38 inhibitor, a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
CN103432156A Medicinal composition of omega-3 fatty acid and B vitamin and application thereof The invention relates to a medicinal composition containing omega-3 fatty acid and B vitamins. The omega-3 fatty acid is selected from long chain polyunsaturated fatty acids, mainly including eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), wherein the content of each component of the two is 100-600 mg; the B vitamin is preferably a folic acid type compound, vitamin B6 or vitamin B12 and the content is 0.01-50 mg. The invention also provides application of the medicinal composition in preparation of a medicament for treating hypertriglyceridemia and preventing or delaying atherosclerosis and related diseases. The medicinal composition has the advantages that a better blood fat lowering effect is achieved, and a vascular endothelium protection effect (mainly acting on a new target point of homocysteine) can also be provided, so that the formation of the atherosclerosis can be prevented and treated cooperatively, and the clinical application of the medicinal composition is superior to the single use of the omega-3 fatty acid. In addition, a patient can conveniently take the medicine.
CN102302472A Enrofloxacin microcapsule and preparation method thereof The invention belongs to the technical field of veterinary medicine, specifically relates to enrofloxacin microcapsule and a preparation method thereof. The enrofloxacin microcapsule is characterized in that: raw materials of the enrofloxacin base microcapsule comprise: 0.1-0.3 parts of enrofloxacin, 0.7-0.9 parts of polyethylene glycol having molecular weight more than 4000, 1.0-1.5 parts of liquid paraffin, 1.8-2.5 parts of ligroin and 0.1-0.15 parts of a non-ionic surfactant. According to the enrofloxacin microcapsule provided by the present invention, the bitter taste of the enrofloxacin is well covered, such that the phenomenon that the livestock do not eat the enrofloxacin due to the bitter taste of the enrofloxacin is overcome. The preparation process is simple; the entrapment rate of the enrofloxacin microcapsule product is high; the product has characteristics of stability, effectiveness and safety, low cost, and is suitable for the industrial production on a large scale.
WO2011006803A8 3-0x0-2, 3, -dihydro-1h-isoindole-4-carboxamides with selective parp-1 inhibition There are provided substituted 3 -oxo - 2, 3 -dihydro- 1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
US7981861 Method of performing angioplasty with a GLP-1 molecule The invention relates to methods for treating a patient suffering from acute coronary syndrome, but who is not suffering from a Q-wave myocardial infarction, comprising administration of a therapeutically effective amount of a GLP-1 molecule. The GLP-1 can be self-administered, and can be administered in one or more doses, as needed, on an intermittent or continuous basis, to optimize metabolism in cardiac tissue and to prevent cardiac damage associated with ischemia.
CN101130062A Segmented intestine targeted drug feeding preparation of brain protein polypeptide and method of preparing the same The invention discloses a colon specific targeting drug-delivery preparation of cerebroprotein polypeptides and its preparing process, wherein the preparation is prepared through coating the drug-containing micro-pellets made from medicinal powder containing cerebroprotein polypeptides components with colon targeting coating layer, or directly loading the drug-containing micro-pellets into the shells of the colon targeting capsule. The process for preparing the colon targeting drug-delivery preparation of the cerebroprotein polypeptides consists of producing drug-containing micro-pellets containing cerebroprotein polypeptides components, then preparing the colon targeting coating liquid, finally coating the drug-containing micro-pellets with the colon targeting coating liquid. The preparation provided by the invention can make the colon release drugs enter blood circulation through colon, thereby avoiding metabolism destruction of the conventional oral preparation peptides drugs on the stomach, as a result, the therapeutic action of the drugs can be sufficiently exploited.
CN102688208A Ornidazole tablet and preparation method thereof The invention discloses ornidazole tablets and a preparation method thereof... The ornidazole tablets (every 1000 tablets) are characterized by comprising 238.5-268.0g of ornidazole, 9.0-11.5g of lactose, 28.0-34.8g of microcrystalline cellulose, 39.3-45.5g of soluble starch, 5.8-6.3g of sodium carboxymethyl starch, 14.2-16.3g of pregelatinized starch, 0.9-1.1g of magnesium stearate and 2.8-3.2g of adhesive (on dry powder basis). The invention solves the problem of that the ornidazole tablets are not protected by any patent in China at present.
WO2007026219A2 Combinations of a 5-ht1b antagonist with a noradrenalin re-uptake inhibitor or a serotonin noradrenalin reutake inhibitor for treating cns conditions The present invention relates to pharmaceutical compositions comprising 5-HT1B antagonists in combination with noradrenaline re-uptake inhibitor (NRI) or serotonin noradrenaline reuptake inhibitor (SNRI) and optionally a pharmaceutically acceptable carrier, and to their medicinal use in treating or preventing CNS conditions such as depression, anxiety, cognitions, ADHD, and comorbid indications.
EP1652536A1 Wound treatment agent comprising a zeolite iod clathrat A wound treatment agent (A1) comprises a zeolite-iodine inclusion compound (c1). An independent claim is included for a wound-stilling material, where (A1) is covered on the side facing towards the wound, by a porous textile fibrous material (preferably non-woven or knitted fabric) and a moisture-permeable sheet. - ACTIVITY : Vulnerary. Physiological saline (45 ml) was admixed with a germ suspension of Staphylococcus aureus to obtain a concentration of 1.5x107> cfu/ml. To this germ suspension, zeolite-iodine complex (10%) (1 g) was added, followed by slight agitation. After different periods of time, 1 ml each was removed, and the number of surviving germs was determined by a plate-casting method in TSA-agar. Incubation was effected at 37[deg]C for 24 hours. The results were: sampling after 1 minutes: strong growth; sampling after 5 minutes: no growth; sampling after 15 minutes: no growth; and sampling after 30 minutes: no growth. Thus, the zeolite-iodine complex released so much iodine under these conditions that all the germs were killed. - MECHANISM OF ACTION : None given.
CN103393606A High-encapsulation-rate wild cactus polysaccharide gelatin microspheres and preparation method thereof The invention relates to high-encapsulation-rate wild cactus polysaccharide gelatin microspheres and a preparation method thereof. The preparation method comprises the steps that: a small amount of gelatin is dissolved into a proper amount of water; a wild cactus polysaccharide solution is added; the materials are sufficiently mixed and pre-emulsified, such that a water-phase solution is prepared; an oil-phase continuous phase is liquid paraffin, and a small amount of tween-80 is added as an emulsifier; on a basis that original stable condition is maintained, the gelatin polysaccharide water phase is slowly added into liquid paraffin, and the mixture is well mixed; after sufficient emulsification, the mixture is rapidly cooled to below 5 DEG C while stirring is continued; glutaraldehyde is added, and curing is carried out for 2h; centrifugation is carried out and precipitate is fetched; residual oil and glutaraldehyde are removed by washing by using isopropanol or ethanol; and lyophilization is carried out, such that microspheres are obtained. With the method, drug load and encapsulation rate of wild cactus polysaccharide microspheres respectively reaches 7.47% and 91.38%. The method has the advantages of simple process, low cost, and high repeatability. The prepared wild cactus polysaccharide gelatin microspheres has round appearance, uniform particle size, good dispersion, high encapsulation rate, good biocompatibility, and good biodegradability.
CN102698013A Tablets for treating traumatic injury and fracture dislocation The invention discloses a group of tablets for treating traumatic injury and fracture dislocation, wherein the tablets are composed of the following raw materials: calcinated natural copper, dragon's blood, Acacia catechu, rehmannia glutinosa, dodder, roasted rhizoma drynariae, dipsacus asper, roasted polygonum multiflorum, deep-fried atractylodes macrocephala koidz, poria cocos, cortex moutan, antler pieces (two branches), cyathnla capitata, safflower, roasted frankincense, immature bitter orange, rhubarb, roasted myrrh, roasted liquorice, Angelica sinensis, roasted Eucommia ulmoides, ligusticum wallichii, elephant hide and deep-fried talc powder.
EP2609925A2 Dermatan sulfate for use in the treatment of pathologies wherein metalloproteinases are involved The present invention describes dematan sulfate obtained from sulodexide for use in the reduction of circulating matrix metalloproteinase (MMPs), in particular MMP-9. Dermatan sulfate is useful for the treatment of pathologies wherein the MMPs are involved, such as cardiovascular disease, cardiovascular disease caused by diabetes, varicose veins, chronic venous insufficiency (CVI), gastrointestinal ulcers, pulmonary disease, and neoplastic pathologies.
WO2008040548A2 Treatment for non-alcoholic-steatohepatitis The present invention provides methods of treating a subject with non- alcoholic fatty liver disease (NAFLD), insulin resistance, obesity or hyperlipidemia, comprising administering to the subject an effective amount of a compound according to Formula (I): or a physiologically acceptable salt thereof.
WO2011133659A3 Inhibitors of hif and angiogenesis Inhibitors of the Hypoxia Inducible Factor (HIF) and angiogenesis and their methods of use including the treatment of cancer, hypoxia related pathologies, disorders leading to ischemia, for example stroke and ischemic heart disease, and non-cancerous angiogenic diseases are provided.
CN102949379A Netilmicin sulfate inhalation powder and preparation method thereof The invention discloses netilmicin sulfate inhalation powder and a preparation method thereof. The powder consists of the following raw materials:, namely netilmicin sulfate or a mixture of the netilmicin sulfate and an amino acid glidant, wherein the weight ratio of the netilmicin sulfate to the amino acid glidant is 10-30:1. The method has the advantages that the preparation technology is simple, no organic solvent or preservative is used in the preparation process, the flowability of the prepared powder is greatgood, the deposit rate at effective parts is high, and the problems that the netilmicin sulfate has high water solubility and cannot be absorbed when isbeing orally taken are solved; and meanwhile, as the inhalation powder is used as a medicine performing a local function, the dosage of administration is obviously reduced, and the occurrence rate of side effects related to an aminoglycoside dosage, such as ototoxicity and renal toxicity is reduced.
US8440827 Photolabile caged transition metal complexes and methods of using the same The present invention provides compounds of Formula I: (I) along with compositions comprising the same and methods of using the same, such as for photodynamic therapy in the treatment of cancer.
WO2009051504A1 Benzo- and pyridopyridazinones with analgesic and antiinflammatory activity Derivatives of phthalazinone and pyridopyridazonone of formula (I) and (II) having practical application as analgesic and antiinflammatory medicaments, in which n is an integer from 1 to 8 for straight or branched alkyl or alkenyl R1 is -NR7R8-COZ M is nitrogen (N) and G = Y = X = carbon (C); R3 = none; G is nitrogen (N) and M = Y = X = carbon (C); R4 = none; Y is nitrogen (N) and M = G = X = carbon (C); R5 = none; X is nitrogen (N) and M = G = Y = carbon (C); R6 = none and the salts of this compounds.
US20100152213 Compound that is a dual inhibitor of enzymes pde7 and/or pde4, pharmaceutical compositions and uses thereof The invention relates to a series of dual inhibitors of enzymes PDE7 and PDE4, having formula (I) and to the use thereof in the production of pharmaceutical compositions for the treatment of inflammatory and/or autoimmune processes.
CN103483345A Phosphoinositide 3-kinase (P13K) inhibitor, pharmaceutical composition containing P13K inhibitor, and application of phosphoinositide kinase inhibitor and pharmaceutical composition The invention discloses a phosphoinositide 3-kinase (P13K) inhibitor, a pharmaceutical composition containing the P13K inhibitor, and application of the P13K inhibitor and the pharmaceutical composition. The P13K inhibitor comprises a pyrimidine compound and a stereoisomer/hydrate/pharmaceutically-acceptable salt thereof. The pyrimidine compound has a general formula I of which the structure is shown in the specification. The P13K inhibitor and the pharmaceutical composition containing the same can be used for inhibiting PI3 Ks and treating proliferative diseases on which the PI3 Ks act. According to the invention, high-effectiveness and high-selectivity inhibitors for treating proliferative diseases on which PI3Ks act can be provided.
WO2008038832A1 Therapeutic agent, detection method and detection kit for breast cancer and ovarian cancer The object is elucidate the role of a PRDM family on cancer and to provide a novel therapeutic agent for cancer associated with PRDM and a method for detection of the cancer. Thus, provided are: a therapeutic agent for breast or ovarian cancer, which comprises an inhibitor of the expression of PRDM14 gene or an inhibitor of PRDM14; and a method for detecting breast or ovarian cancer in a subject based on the level of the expression of PRDM14 gene in a biological sample collected from the subject.
CN1795847A Liposome of Nitrocaphane and preparation method A nitrocaphane lipid for suppressing tumor with broad spectrum and low poison is proportionally prepared from nitrocaphane, phosphatide, cholesterol and supporting additive by alcohol filling method, film dispersing method, reverse-phase evaporation method, extruding out method, or mechanical method.
CN1850067B In vivo oxygen-supply solution for injection, and its preparing method and use The present invention relates to an internal oxygen supply solution for injection. In particular, it relates to a solution type injection made up by using one oxygen-supplying main component and injection solvent formed from one or more than one polyhydroxy-alcohol. Said invention also provides its preparation method.
US20120165336 Color Change Time Indicator for Packaging System Disclosed in certain embodiments is a pharmaceutical packaging system comprising: a receptacle comprising an openable seal for accessing the interior of the receptacle; a pharmaceutical dosage form contained in the receptacle; and an activatable color-changing material, wherein upon activation, the material exhibits a visually discernible color change upon the lapsing of a predetermined time period.
EP2219546A1 Endoscopic mucosal resectioning using purified inverse thermosensitive polymers One aspect of the invention relates to use of a composition comprising a purified inverse thermosensitive polymer in an endoscopic procedure for gastrointestinal mucosal resectioning in a mammal. Another aspect of the invention relates to a method of gastrointestinal mucosal resectioning, comprising administering submucosally to a region of a gastrointestinal mucosa in a mammal an effective amount of a composition comprising a purified inverse thermosensitive polymer; and surgically resecting said region of gastrointestinal mucosa. Yet another aspect of the invention relates to a kit for use in gastrointestinal endoscopic mucosal resectioning in a mammal, comprising a composition comprising a purified inverse thermosensitive polymer; a syringe; and instructions for use thereof.
US7265156 Medicinal association of a biguanine and a carrier, for example metformin and arginine The present invention relates to a compound of formula III, method of making the same and its use in the treatment of diabetes.
CN101544634B 2-phenyl-3-substituted pyrazolo[1,5-a]pyridine derivatives, preparation method and application thereof The invention relates to pharmaceutical compounds (I) for treating diseases such as tumor and viruses, a preparation method and application thereof, wherein the definitions of R1, R2, R3 and R4 are described as description. The invention also discloses pharmaceutical compositions consisting of compounds taken as active ingredients I against tumor and viruses or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable carriers, excipients or diluting agents.
CN102631528A Chinese patent drug composite for treating acute urticaria The invention discloses a Chinese patent drug composite for treating acute urticaria and belongs to the technical field of medicines for treating urticaria. The technical scheme adopted by the invention is as follows: the Chinese patent drug composite is characterized by being prepared from the following materials in parts by weight: dittany bark, root-bark of tree peony, herba schizonepeta, divaricate saposhnikovia roots, roots of rehmannia, angelica sinensis, root of common peony, radix sophorae flavescentis, herba siegesbeckiae, golden cypress, rhizoma anemarrhenae, rhizoma atractylodis, belvedere fruit, talcum powder, peach kernels, safflowers, prepared rhizome of rehmannia, radix angelicae pubescentis, the root of fangji, ligusticum chuanxiong hort, notopterygium roots and raw liquorice. Compared with the prior art, the Chinese patent drug composite provided by the invention can be used for eliminating diseases of patients and promoting the physical and psychological health, and meanwhile has the obvious practical characteristics and obvious improvements of low treatment cost, convenience for patients to take, rapid curative effect taking, and no side effects in treating acute urticaria.
US20060235132 Method of preparing poly(vinyl pivalate) by low temperature suspension-polymerization of vinyl pivalate, and poly(vinyl pivalate) and poly(vinyl alcohol) prepared using same Poly(vinyl pivalate) exhibiting a high syndiotacticity and a high molecular weight is prepared through suspension polymerization of vinyl pivalate at low temperatures. Furthermore, poly(vinyl pivalate) microspheres with a high syndiotacticity is prepared for use as a precursor for PVA with a high molecular weight and a high syndiotacticity through suspension polymerization of vinyl pivalate at 20 to 70° C. with the use of azobisdimethylvaleronitrile as an initiator. In addition, poly(vinyl pivalate) is separated using a dispersing agent and a precipitating agent to thereby prepare poly(vinyl pivalate) microspheres with various sizes and a uniform size distribution. The poly(vinyl pivalate) microspheres are suspended in an aqueous alkali soloution such that only the surface thereof is saponified to PVA. In this way, embolic particles with a spherical shape are obtained to be useable as an embolic material for embolotherapy.
CN1679622A Use of sodium selenite in preparing medicine for osseous arthritis An application of sodium selenite in preparing the medicines for preventing and treating osteoarthritis is disclosed. Its advantages are high curative effect and no toxic by-effect.
CN102091097A Washing-free puerpera perineum medical-care gel and preparation method thereof The invention relates to washing-free puerpera perineum medical-care gel, which comprises the following components: 0.1 to 5 percent of water soluble chitosan, 0.5 to 5 percent of propolis extract, 0.3 to 1 percent of halogenated biphenyl ether or biguanide fungicide, 0.3 to 1.5 percent of water soluble polymer gel material, 0 to 7 percent of solvent, 0.1 to 1 percent of triethanolamine, 0.05 to 0.5 percent of chelating agent, 0.05 to 0.5 percent of emollient and the balance of distilled water. The washing-free puerpera perineum medical-care gel is prepared by uniformly mixing the components.The washing-free puerpera perineum medical-care gel has the perineum-cleaning, dirt-removing, antibacterial, antiviral, anti-inflammatory, local inflammation diminishment promoting, blood circulationpromoting, bleeding stopping and wound healing promoting functions.
US20080033007 Substituted Tetrahydroisoquinoline Compounds for Cancer Therapy Disclosed are compounds that are effective for selectively killing cancer cells. Compounds have been demonstrated to be especially effective for killing glioma cells, while exhibiting low toxicity to normal cells.
US20070249657 1-Aza-Bicyclo3.3.1Nonanes The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
WO2007037560A9 Therapeutic or diagnostic application of sgk2 gene It is intended to provide a therapeutic agent for cancer containing an expression inhibitor or activity inhibitor of SGK2 protein; a method for screening a compound which can be used as an active ingredient of such a therapeutic agent; an antibody against the SGK2 protein; a diagnostic agent for cancer/a diagnostic method for cancer using the antibody and the like.
EP1553933A1 Medicine comprising a thiourea for use as depigmenting agent or anti-mutagenic and anti-carcinogenic agent The invention concerns a medicine or a cosmetic composition comprising at least one thiourea of general formula (I), or at least one of its monooxide or dioxide derivatives of general formulae (IIa), (IIb) and (III), or mixtures thereof. This medicine is advantageously used for inhibiting tyrosinase, inhibiting melanin synthesis, for lightening or depigmenting the skin or for eliminating age spots and as antimutagenic and anti-carcinogenic agent.
US20110082097 Amino acid composition for improving glucose tolerance Disclosed are compositions, including low-calorie beverages or liquids, comprising isoleucine, leucine, valine, cysteine, and methionine, in specified amounts, weight ratios, or both. The compositions are especially useful in treating individuals afflicted with impaired glucose tolerance or diabetes.
WO2014039434A1 Alkoxy pyrazoles as soluble guanylate cyclase activators The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
US7122554 Sexual disorders therapy; hypotensive agents; chronic obstructive pulmonary disease; congestive heart failure; asthma; antiallergens Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.
US20080096850 Exposing Grampositive bacteria of vagina to a synergistic mixture including hexachlorophene, benzyl paraben, benzyl salicylate, a benzophenone, chlorophene, 2,4-diaminodiphenylamine, dichlorophene, HC Green No. 1, HC Orange No. 1, HC Red No. 1, isopropylbenzyl salicylate, and phenyl salicylate; tampons Methods for inhibiting the production of TSST-1 from Gram positive bacteria are disclosed. The methods comprise exposing the Gram positive bacteria to compounds capable of inhibiting the production of TSST-1 from the Gram positive bacteria.
US20080280858 Method of creating crystalline substances Process for preparing a cocrystal of an active substance and a cocrystal former, the process involving precipitating the active substance and the cocrystal former together from solution or suspension, in the presence of a supercritical or near-critical fluid, in particular using a GAS, SAS, SEDS or SAS-EM process. The invention also provides a cocrystal prepared using such a process, and its use as a seed crystal in a subsequent process for precipitating a cocrystal of an active substance and a cocrystal former.
WO2009101210A1 Pharmaceutical composition for use in the treatment or prevention of osteoarticular diseases The present invention is related to a pharmaceutical composition for the acute and/or chronic treatment (or prevention) of osteoarticular diseases, comprising possibly an adequate pharmaceutical carrier or diluent a polysaccharide and/or a glycosaminoglycan an anti-inflammatory agent and stem cells.
US20130096120 Apoptosis-induced agents for the treatment of cancer and immune and autoimmune diseases Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
EP1503763A1 Therapeutic 1,2,3,6-tetrahydropyrimidine-2-one compositions and methods therewith A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one cold receptor agonist in a therapeutically effective amount. The composition preferably further comprises one or more pharmaceutically active drugs such as an anti-inflammatory glucocorticosteroid, a sympathomimetic amine decongestant, an antihistamine, a local anesthetic, menthol or a menthol analog, an immunosuppressant, and mixtures thereof. The cold receptor agonist may be represented by the general formula (1)-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 is -hydroxy, -chloro, - fluoro, -alkyl, -acetoxy, -trifluoromethyl ; and R2 is -nitro, -chloro, -fluoro, -alkyl, -trifluoromethyl. Therapeutic compositions of the invention elicit long-lasting cooling or soothing, particularly when formulated for delivery to suppress the sensations of itch and pain, such as for delivery to inflamed skin, to the mucous membranes of the eyelids, of the anogenital areas and of the airways, and to the enteric mucosa.
EP2218718A1 Amorphous form of heterocyclic compound, solid dispersion and medicinal preparation each comprising the same, and process for production of the same [PROBLEMS] The object is to improve the absorbability of a heterocyclic compound including s-triazine and a pyrimidine derivative in vitro. [MEANS FOR SOLVING PROBLEMS] Disclosed is, for example, an amorphous body of a heterocyclic compound as represented by the general formula (I) [wherein each of R's and others is as defined in the description] including s-triazine and a pyrimidine derivative, or a hydrate, a solvate or a pharmaceutically acceptable salt of the heterocyclic compound. Also disclosed is a process for producing the amorphous body Further disclosed are: a solid dispersion comprising the amorphous body; and a medicinal preparation comprising the solid dispersion.
EP1581528B1 Piperidinyl-thiazole carboxylic acid derivatives as angiogenesis inhibitors This invention relates to compounds of formula (I) and (II) that are useful in treating vascular endothelial growth factor (VEGF)-mediated disorders, particularly endometriosis and acute macular degenerative disorder. The invention also relates to a topical system for the treatment of acute macular degenerative disorder comprising a VEGF inhibitor.
CN1853632A Herba fibraurae recisae soft capsules and production thereof A fibrauretin softgel is composed of the liquid medicine prepared from fibrauretin, plant oil and suspending aid and the softgel shell prepared from gelatin, glycerin and water through pre-treating, proportional mixing and die pressing.
US20080274104 Targeting a Secreted Pro-Apoptotic Factor for Cancer Therapeutics The present invention concerns targeting a cell death factor associated with cancer. More specifically, an apoptosis-inducing factor is targeted to prevent destruction of non-cancerous cells. The factor may be a lipocalin molecule, and in specific embodiments its secretion and/or the secreted form is targeted by an inhibitory agent, such as an antibody, small molecule, antisense RNA, or siRNA, for example.
CN1736394A An anti-AIDS injection and preparation process thereof The invention relates to an intra-vascular instillation type injection having substantial effect for treating AIDS, wherein its preparing process comprises cantharis selection, disintegrating, cantharidin extraction, cantharidin degreasing, sodium cantharidate synthesis, refining, synthesis, encapsulation and sterilizing.
CN101229120A Sustained release implant for treating solid tumors The invention discloses a sustained-release implant used for curing solid tumors, being characterized by comprising Revlimid in certain amount for anticancer and sustained-release auxiliary materials, the solid tumors comprise brain tumor, liver cancer, lung cancer, esophageal cancer, gastric cancer, breast cancer, pancreatic cancer, thyroid cancer, nasopharyngeal cancer, ovarian cancer, endometrial cancer, cervical cancer, renal cancer, prostate cancer, bladder cancer, colon cancer, rectal cancer, skin cancer, head and neck cancer, primary or secondary cancer, sarcoma or carcinosarcoma caused by peripheral nervous system, mucosa, glands, vessels, bone tissues and lymph nodes, the sustained-release auxiliary materials are mainly biological soluble, degrading and absorptive polymer, when the material is being degraded or absorbed, carmustine can be slowly released into parts of tumor, so the systemic toxicity react can be obviously reduced, at the same time the material can also be used for keeping effective drug concentration in parts of tumor, placing the sustained-release implant on parts of tumor can not only reduce the systemic toxicity react of carmustine but also selectively improve the drug concentration in parts of tumor, so as to improve the treatment outcome of non-operative treatments such as chemotherapeutic drugs and radiotherapy.
US20110177096 Use of gpr151 modulators for the treatment of pain The present invention relates to nucleic acid arrays used to detect genes which are up or down regulated following a pain stimulus in a mammal. It further relates to the use of GPR151 in methods to detect pain or evaluate the effect of a compound on the level of pain in a mammal. Other aspects of the invention concern a method for screening pharmaceuticals, methods for the treatment of pain and a pharmaceutical composition comprising a GPR151 modulator for the treatment of pain.
WO2014097038A1 CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS The present invention provides compounds of formula (I), wherein the variables R1, R2, R5 and b are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
WO2012122921A1 Salt form of hydroxyphenylalanine kinase inhibitor The present invention pertains to acidic adduct salts of (Z)-N-[2-(diethylamino)ethyl]-2-methyl-7-(1,2-dihydro-5-fluoro-2-oxo-3H-indol-3-ylene)-4,5,6,7-tetrahydro-1H-indol-3-carboxamide, selected from L-malate, hydrochloride, phosphate, L-tartrate, benzene sulfonate, sulfate, methanesulfonate, succinate, citrate, fumarate, p-toluenesulfonate, hydrobromate, L-mandelate, lactate, acetate and maleate, and the use of the above salt compounds for preparing pharmaceuticals.
EP2398805A1 (+)-morphinanium quaternary salts and processes for their production The present invention provides (+)-morphinanium quaternary salts. The invention also provides processes for producing (+)-morphinanium quaternary salts from tertiary N-substituted (+)-morphinan compounds.
US20080312245 Methods and compositions for treating acne and other infectious diseases The present invention provides a composition comprising metronidazole, ketoconazole, and lincomycin and methods of treating infectious skin diseases such as acne by topically administering the composition.
US20130203767 Treatment of Pulmonary Hypertension This invention relates to the use of certain cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.
WO2006085330A3 Use of protein tyrosine kinase inhibitors for the treatment of leiomyomas Pharmaceutical compositions containing epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors or natural protein kinase inhibitors and use thereof for the treatment of leiomyomas are disclosed.
EP1789068B1 Composition and use for prevention or treatment of stomatitis A composition and a method effective in preventing or treating stomatitis are presented. The composition contains glutathione or a pharmaceutically acceptable salt thereof and/or orotic acid or a derivative thereof or a pharmaceutically acceptable salt thereof is provided.
US20090131480 Dihydropyridine Compounds for Neurodegenerative Diseases and Dementia The invention provides methods for treating and/or preventing cognitive impairments, dementia, or neurodegenerative diseases and disorders (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis) in patients by administering therapeutically effective amounts of an AMPA receptor antagonist (e.g., 1,2-dihydropyridine compounds) and therapeutically effective amounts of nootropics (e.g., cholinesterase inhibitors) to patients. The invention also provides combinations, commercial packages, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists (e.g., 1,2-dihydropyridine compounds) and therapeutically effective amounts nootropics (e.g., cholinesterase inhibitors). The 1,2-dihydropyridine compound may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. The cholinesterase inhibitor may be, for example, donepezil.
US20080063725 Reservoir type, modified release of active principle; crush resistant; resists immediate dose dumping in ethanol; prevents abuse, misuse, drug addiction related behavior with stupefacients, analgesics or narcotics; microparticles coated with water-insoluble cellulose derivatives, nitrogenous copolymers Modified-release multimicroparticulate pharmaceutical form capable of maintaining the modified release of the active principle in an alcoholic solution and of resisting attempts at misuse.
WO2006039545A3 Use of parp-1 inhibitors for protecting tumorcidal lymphocytes from apoptosis Method and composition for protecting tumorcidal lymphocytes including cytotoxic lymphocytes and NK cells from apoptosis and down regulation are provided. The method and composition include the administration of an effective amount of a PARP-1 inhibitor to a population of cytotoxic T lymphocytes and NK cells in the presence of monocytes or macrophages. In some embodiments, the method and composition additionally include the administration of a reactive oxygen metabolite (ROM) production or release inhibitory compound. Methods of treating cancer, viral diseases, and inflammatory diseases with a PARP-1 inhibitor are likewise provided.
US20100047321 Silver antimicrobial composition and use Aqueous silver-containing composition is designed for use as an antimicrobial agent on fibers and fabrics. This composition includes silver halide particles, gelatin, and an additive that includes an N-heterocyclic acid having a pKa of from about 4 to about 9. The additive improves the redispersibility and shelf-life of the composition.
US20100068242 Medical Devices for Localized Drug Delivery In certain embodiments, the invention relates to an implantable medical device that includes a body having an internal cavity. Receptor sites in the internal cavity may be adapted to repeatedly bind to, temporarily hold, and release an active agent. An opening may extend through the body and into the internal cavity to allow the active agent into and out of the internal cavity. This opening may be sized and shaped to prevent blood cells from entering the internal cavity through the opening while allowing the active agent to enter and/or exit the cavity via the opening. A polymeric structure may be located in the internal cavity. This polymeric structure may include artificial receptor site mimics for the active agent.
CN101827594A Combination therapy for reducing side effects using cannabinoid receptor ligands The present application describes a method of treating conditions treatable with a CB2 cannabinoid receptor agonist with reduced CB1- mediated side effects using a combination therapy comprising a CB2 agonist and a CB1 ligand, which can be a CB1 antagonist or a CB1 inverse agonist.
CN101248048A Imidazole based LXR modulators Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R<1>, R<2>, R<21>, R<3>, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
EP2241557A1 Chinoxalin derivatives and use thereof for treating malignant and benign tumour illnesses Quinoxaline compounds (I) and their salts, hydrates, solvates, racemates, enantiomers and/or diastereomers, or in the form of mixtures of the enantiomers and/or diastereomers, in the form of the tautomers and their polymorphic forms are new. Quinoxaline compounds of formula (I) and their salts, hydrates, solvates, racemates, enantiomers and/or diastereomers, or in the form of mixtures of the enantiomers and/or diastereomers, in the form of the tautomers and their polymorphic forms are new. X : O or S; R 1H, 1-12C alkyl (optionally substituted), CN or halo; R 2, R 3H or 1-12C alkyl (optionally substituted); R 41-12C alkyl, cycloalkyl, heterocyclyl, (hetero)aryl, alkylaryl or alkylheteroaryl (all optionally substituted) or H; and R 5-R 81-12C alkyl or (hetero)aryl (all optionally substituted), H, halo, CN, OH, 1-12C alkoxy, amino, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonylamino or alkoxycarbonylaminoalkyl, where the substituents are F, Cl, Br, I, CN, CF 3, NH 2, NH-alkyl, NH-aryl, N(alkyl) 2, NH-CO-alkyl, NH-CO-aryl, NH-CO-heteroaryl, NH-SO 2-alkyl, NH-SO 2-aryl, NH-SO 2-heteroaryl, NH-CO-NH-alkyl, NH-CO-NH-aryl, NH-CO-NH-heteroaryl, NH-C(O)O-alkyl, NH-C(O)O-aryl, NH-C(O)O-heteroaryl, NO 2, SH, S-alkyl, OH, OCF 3, O-alkyl, O-aryl, O-CO-alkyl, O-CO-aryl, O-CO-heteroaryl, OC(O)O-alkyl, O-C(O)O-aryl, O-C(O)O-heteroaryl, O-CO-NH-alkyl, O-CO-N(alkyl) 2, OCO-NH-aryl, O-CO-NH-heteroaryl, OSO 3H, OSO 2-alkyl, OSO 2-aryl, OSO 2-heteroaryl, OP(O)(OH) 2, alkyl-P(O)(OH) 2CHO, CO 2H, C(O)O-alkyl, C(O)O-aryl, C(O)O-heteroaryl, CO-alkyl, CO-aryl, CO-heteroaryl, SO 3H, SO 2-NH 2, SO 2-NH-alkyl, SO 2-NH-aryl, SO 2-NH-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl, where the radicals alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl (all optionally substituted). With the proviso that at least one of the substituents R 5-R 8is optionally substituted (hetero)aryl radical. An independent claim is included for a composition comprising (I). [Image] - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : None given.
WO2013105056A1 Pyrrolidine- substituted flavone derivatives for prevention or treatment of oral mucositis The present invention relates to the pyrrolidine substituted with flavone derivatives, represented by the compounds of Formula (I) (as described herein) or pharmaceutically acceptable salts, solvates, stereoisomers or diastereoisomers thereof or pharmaceutical compositions containing the compounds of Formula (I) for use in the prevention and/or treatment of oral mucositis caused by cancer therapy such as radiation therapy.
US7112673 Dibenzo [b,f]azepine intermediates The invention relates to new processes for the preparation of the pharmaceutical oxcarbazepine, as well as novel intermediates prepared by or used for said processes, and the preparation of said intermediates.
CN101269204A Cow-bezoar bolus for resurrection and preparation method thereof The invention provides a dripping bezoar chest functioning pill and a preparation method thereof, which is prepared by mixing the medical components, which are extracted from eleven materials of bezoar, concentrated powder of cornu bubali, musk, pearls, cinnabar, realgar, coptis, scutellaria, gardenia, radix curcumae, and borneol with substrate by the ration of 1 to 1-4, and then conducting the steps of melting, dripping, drying and coating. The medicine of the invention takes effect quicker than the traditional bezoar chest functioning pill with less dosage, can be swallowed, kept in mouth, be taken from nasal delivery with better pharmacological effect.
CA2221075C Use of aminoalcohol derivatives in the treatment of liver disease The present invention discloses a method for the treatment of liver diseases, comprising administering an effective amount of an aminoalcohol of the following formula (1) or a salt thereof: wherein R1 represents a hydrogen atom or a phosphono group, R2 represents a hydrogen atom or a group -(CH2)n-OR1, and n represents an integer between 2 and 5 inclusive. The present invention also relates to the use of the compound in the manufacture of a remedy for the treatment of liver diseases. This compound exhibits hepatocyte proliferation activity and liver disorder restoring effect, and thus is useful for the treatment of acute hepatitis, chronic hepatitis, hepatic cirrhosis, etc.
WO2008009963A2 Pyrimidine derivatives as modulators of parathyroid hormone receptors The present invention is concerned with pyrimidine derivatives, their intermediates, uses thereof and processes for their production. In particular, the present invention relates to parathyroid hormone (PTH) and parathyroid hormone related protein (PTHrp) receptor ligands, (PTH-I or PTH/PTHrp receptor ligands). The invention also relates to methods of preparing such ligands and to compounds which are useful as intermediates in such methods.
CA2272439C A process for the preparation of 13-cis-retinoic acid A process for the synthesis of 13-cis-retinoic acid of Formula I (see formula I) with high purity and stability, without using heavy metals at any steps, starting from vinyl-beta-ionol prepared from ionone and vinyl magnesium halides.
WO2012099381A2 Preparation method of intermediate of sitagliptin The present invention provides a method which enables the simple, economical and high-yield production which is a key intermediate of antidiabetic drug Januvia.
WO2012087047A3 Percutaneous absorption preparation containing rivastigmine Disclosed is a percutaneous absorption preparation for treatment of dementia that comprises rivastigmine or its pharmaceutically acceptable salt as an active ingredient, a styrene-isoprene-styrene block copolymer, a tackifier resin, and a plasticizer, which preparation contains a small amount of rivastigmine but allows a sufficient amount of the active ingredient penetrated into the skin to achieve an effective treatment of dementia.
WO2010127608A1 Heterocyclic substituted acardite derivates and use thereof A heterocyclic substituted acardite derivate and use thereof; namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole, pyrimidine. The substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or some of hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or some of hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.
WO2009081892A1 Novel catechol derivative, pharmaceutical composition containing the same, and use of those Disclosed is a compound represented by the general formula (I) below which has a strong COMT inhibitory effect, or a pharmacologically acceptable salt thereof. Also disclosed are a pharmaceutical composition containing such a compound or a pharmacologically acceptable salt thereof, and a use of those. (In the formula, R1 and R2 independently represent a hydrogen, a lower acyl, a lower alkoxycarbonyl or the like; R3 represents a halogen, a halo-lower alkyl, a cyano or the like; R4 represents a hydrogen, a lower alkyl or the like; and R5 and R6 independently represent a hydrogen, an alkyl, a cycloalkyl, a heterocycloalkyl, a halo-lower alkyl, an optionally substituted aryl, an optionally substituted heteroaryl or the like.)
US20110124684 Aminopyrazole triazolothiadiazole inhibitors of c-met protien kinase The present invention relates to compounds of formula I, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders.
US20110160307 Compositions and Methods for Treating Hemorrhagic Conditions A method of treating a hemorrhagic condition in a subject in need thereof, comprising administering a composition comprising a therapeutically effective amount of Dencichine, a co-solvent, a dispersion supporter, and optionally a cryoprotectant. Compositions and formulations comprising a solid dispersion composition of Dencichine and methods for preparation of same are also described.
WO2012125772A3 Oral formulations for promoting cellular purification An oral formulation includes a plurality of agents that promote cellular detoxification. Agents can be included that modulate expression of Nrf2-associated genes upon ingestion of the oral formulation by a subject, wherein the Nrf2-associated genes include at least one gene encoding intrinsic antioxidants, and at least one gene encoding cellular detoxifiers. In addition, at least one of the plurality of agents attenuates inflammation.
CN102908311A Tolfenamic acid injection and preparation method and application thereof The invention discloses a tolfenamic acid injection and a preparation method and application thereof. The tolfenamic acid injection disclosed by the invention comprises a main drug, a cosolvent, a pH regulator, a preservative agent and a local analgetic agent. The tolfenamic acid injection disclosed by the invention is safe and convenient to use and controllable in quality; the preparation process of the tolfenamic acid injection is stable, suitable for industrial production and low in cost; and the tolfenamic acid injection enriches veterinary clinical drugs and has obvious effect if being used for treating arthritis, arthritic pain and surgical pain of dogs, cats and the like.
CN102008432A Sodium demethylcantharidate medicinal composition for injection and preparation method thereof The invention relates to a sodium demethylcantharidate injection, which comprises sodium demethylcantharidate, cysteine hydrochloride, tertiary butyl p-hydroxy anisole and propylene glycol surfactants in effective curative dose. In the composition, the stability of products is improved greatly by adopting a special process and taking the cysteine hydrochloride and the tertiary butyl p-hydroxy anisole as a combined antioxidant. The invention also discloses a method for preparing the medicinal composition.
US7094805 Total synthesis of merrilactone A This invention provides a total synthesis of Merrillactone and Merrilactone analogues for use as neurotrophic agents in the treatment of neurodegenerative diseases. The invention also provides intermediates for use in the synthesis of Merrilactone and its analogues.
US20130109655 Method for mitigating of Prostaglandin E2 reducing side effects of non-steroidal anti-inflammatory drugs This invention relates to a method of mitigating side effects of non-steroidal anti-inflammatory drugs, specifically to administration of a pyridine derivative to mitigate and/or prevent prostaglandin e2 reducing side effects of non-steroidal anti-inflammatory drugs. Also provided is the use of a pyridine derivative in the preparation of a medicament for the reduction of said side effects of non-steroidal anti-inflammatory drugs, and a pharmaceutical composition comprising a non-steroidal anti-inflammatory drug and a pyridine derivative.
US7871997 Potency against gram-positive bacteria, methicillin-resistant Staphylococci aureus (MRSA), methicillin-resistant Staphylococci epidermitis (MRSE). This invention provides cephalosporin compounds and salts thereof. Such compounds are useful for preparing cross-linked glycopeptide-cephalosporin antibiotics.
CN101244188A Compound Chinese aloe tablet and preparation thereof The invention relates to a compound aloe tablet as well as the preparation method. The compound aloe tablet is a tablet preparation which uses aloe, indigo, vermilion and amber as the raw material and is made via mixing, palletizing, finishing granule, blending and sheeting after respectively processing. The compound aloe tablet has the functions of removing heat from the liver, relieving constipation and claming mood and an obvious curative effect for treating big heart-fire and liver-fire, constipation, abdominal distention, stomach pain, irritation and insomnia.
CN101378748B Pharmaceutical composition having a ruthenium oxalato compound and method of using the same A pharmaceutical composition comprising one or more of the following ruthenium oxalate compounds Formulae (I , II , III , and IV) as an active ingredient . The pharmaceutical composition can be used for the treatment of viral-infected patients or prophylactic treatment of patients at risk from viral infection .
EP2017337A1 Human tumor necrosis factor receptors A human TNF receptor polypeptide and two splice variants thereof and DNA (RNA) encoding such polypeptides and a procedure for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing such receptor polypeptides for screening for antagonists and agonists to the receptors and for ligands for the receptors. Also disclosed are methods for utilizing such agonists to inhibit the growth of tumors, to stimulate cellular differentiation, to mediate the immune response and anti-viral response, to regulate growth and provide resistance to certain infections. The use of the antagonists as a therapeutic to treat autoimmune diseases, inflammation, septic shock, to inhibit graft-host reactions, and to prevent apoptosis is also disclosed. Also disclosed are diagnostic assays for detecting mutations in the nucleic acid sequences and the polypeptides encoded thereby.
CN101342281A Medicine for treating prostatosis and method for preparing same The present invention discloses a medicine which is used for treating prostate diseases, and is prepared by raw materials of the following weight portions: 3 to 8 portions of borneol, 3 to 8 portions of centipede, 3 to 6 portions of pangolin, 3 to 6 portions of agilawood, 3 to 10 portions of camphor, 3 to 6 portions of Chinese goldthread, 3 to 6 portions of clove, 3 to 8 portions of pinellia, 0.5 to 4 portions of moschus, and 50 to 150 portions of fresh cocklebur. The medicine has practical effects and excellent curative effects on the treatment of prostate diseases, and can be easily used through ordinarily pasting without infection or sequelae. Moreover, the preparation process is simple and feasible; the raw materials for preparing the medicine have a wide source; and the cure rate of the medicine reaches to 98 percent.
WO2014066318A1 Combination therapies for the treatment of alzheimer's disease and related disorders The present invention relates to combination therapies for treating Alzheimer's disease or an amyloidosis-associated pathological condition comprising co-administering a therapeutically effective amount of a first compound, and a therapeutically effective amount of a second compound. In certain embodiments, the first compound or the second compound inhibits AB peptide polymerization; is an anti-inflammatory; improves cognitive function, mood, or social behavior; is associated with Tau or alpha-synuclein; or regulates amyloid peptide washout.
EP2085394A2 Metronidazole derivatives as antiparasitic agents 2-methyl-5-nitro-imidazolyl compounds with the general formula I, II or III: wherein one of the groups R1, R2, R3, R4, R5 is selected from an aldehyde and a 5- or 6-membered aromatic heterocylic group having 1 to 3 heteroatoms selected from N, O, S wherein the aromatic heterocylic group is optionally substituted and is optionally fused with a benzene ring that is optionally substituted; and each of the other groups R1, R2, R3, R4, R5 is independently selected from hydrogen, alkyl, alkenyl, alkoxy, amino, alkylamino, dialkylamino, aryl, aralkyl, carboxyl, carboxylic ester, cyano, amido, bromo, chloro, fluoro, alkylamido and heterocyclic optionally substituted; R6 is selected from - SO2-R16, -(CH2)n-R17; R16 is a heterocylic group optionally substituted; R17 is a heterocylic group optionally substituted; n is selected from 1 to 5; R7 is selected from C2-C10 alkyl, aryl optionally substituted, heterocyclic optionally substituted, alkenyl and C2-C4 hydroxyalkyl; R8, R9, R10, R11, R12, R13, R14, R15 are each independently selected from hydrogen and alkyl; the optionally substituted aryl, heterocyclic, aromatic heterocyclic groups and benzene rings are optionally substituted with one or more groups independently selected from alkyl, alkenyl, alkoxy, amino, alkylamino, dialkylamino, carboxyl, carboxylic ester, cyano, amido, bromo, chloro, fluoro and alkylamido. These compounds are used as antiparasitic and antibacterial agents.
CN101513404A Medicament compound for treating digestive disease and the method for preparing the same The invention discloses a medicament compound for treating digestive disease, wherein the weight ratio of omeprazole to troxipide as active ingredient is 1:1-1:10. The compound preparation can treat gastric ulcer, duodenal ulcer, acute and chronic gastritis, gastroesophageal reflux, functional dyspepsia, and the like. The compound preparation consisting of omeprazole and troxipide good in treating effect compared with a single medicament.
US20110217277 Drug or dermatological composition containing an avocado peptide extract for treating and preventing pruritus The invention relates to a drug or a dermatological composition containing an avocado peptide extract for treating and/or preventing pruritus, in particular gravidic pruritus, pruritus sine materia, pruritus in newborns, and pruritus originating from a drug.
US20090022686 Pharmaceutical compositions for the treatment of systemic inflammatory response syndrome The present invention relates to the use of certain benzimidazoles for preparing a pharmaceutical composition for the treatment of systemic inflammatory response syndrome and particularly sepsis.
CN101732583A Magnetic therapeutic plaster for activating blood circulation, removing blood stasis and inducing menstruation to relieve menalgia and preparation method The invention discloses a magnetic therapeutic plaster for activating blood circulation, removing blood stasis and inducing menstruation to relieve menalgia and a preparation method. The magnetic therapeutic plaster is prepared from musk, rhubarb, amber, frankincense, myrrh, Chinese angelica, pangolin, dipsacus root, Indian iphigenia bulb, red paeony root, dahurian angelica root, Dragon's blood, ginger, asarum, gamboge, diverse wormwood herb, saffron, Sanchi, zanthoxylum husk, schizophragma integrifolium, Chinese Paris rhizome, tall gastrodia tuber, honeycomb, yellow lead, menthol, common threewingnut root and calomel according to a certain proportion through steps of oil immersion, decocting, fire and gas removal, and the like. The magnetic therapeutic plaster has no toxic or side effect, can achieve good treatment effect on diseases such as waist and leg joint sore of rheumatism and rheumatoid, physique pain of hyperosteogeny, female dysmenorrhea and the like, and has the advantages of high treatment effect, short treatment course and quick response.
CN101024622A Theanine amino-acid salt, its preparing method and use The invention relate to an organic salt compound of theanine, the manufacturing method and the usage. It supplies theanine-lysine salt and theanine- arginine salt. It has the biology activity of theanine and corresponding amino acid. It has widely application value in medicine, health products and cosmetics.
US20100160306 Acylated Piperidine Derivatives as Melanocortin-4 Receptor Agonists Certain novel 4 alkyl substituted N acylated piperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
US6849639 Anticancer agents, antiinflamatory agents, osteoporosis, atherosclerosis The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as a αvβ3, αvβ5, αvβ6, α5β1 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
WO2010007788A1 Glycyrrhetinic acid derivative and use thereof Disclosed is a gap junction inhibitor which is more practically useful compared with carbenoxolone. Also disclosed is a novel glycyrrhetinic acid derivative. The glycyrrhetinic acid derivative is represented by general formula (1) or (2).
WO2012005568A1 Nutritional composition for the stimulation of muscle protein synthesis The invention relates to the use of an anabolic amino acid derivative stimulus acting in combination with vitamin D for the manufacture of a medicament or nutritional composition for the prevention and/or treatment of a loss of any one of muscle mass, muscle strength, muscle function, and physical function, or any combination thereof, in an adult mammal.
WO2009115023A1 A anthocyanins phospholipid complex and the preparative method thereof The present invention discloses a phospholipid complex with anthocyanins, wherein the ratio between anthocyanins and phospholipid is 1:1-20 by weight, and anthocyanins can be selected from cyanidin glycoside, or extracted from grape, black rice, bilberry, black currant, hawkthorn, mulberry. The present invention also discloses a method for producing the anthocyanins phospholipid complex: dissolving the mixture of anthocyanins and phospholipid in organic solvents with lower dielectric constant, evaporating the solvents to obtain the anthocyanins phospholipid complex. The anthocyanins phospholipid complex in the present invention can possess high liposolubility, favourable resorption, good bioavailability and can be formulated into emulsion.
US20070286895 Wound dressing The invention provides for the use of an effective amount of silver in the manufacture of a wound dressing comprising an anionic polymer, which dressing, when applied to the wound, gives a controlled release of ionic silver into the wound fluid for the prevention of staining of the underlying tissue.
US20100291168 Antimicrobial formulations comprising a combination of a pyridine thiol and a bis-quinolinium salt An antimicrobial formulation containing a pyridine thiol and a bis-quinolinium salt which contains a cation of formula (I) below: wherein n is an integer from 3 to 18. The formulation may in particular be used for the treatment of a bacterial condition, more particularly acne or body odour. It is suitably applied topically.
CN102000041A Furadantin capsule containing quick-release component and slow-release component and preparation method thereof The invention relates to the field of medicine preparation, in particular to a furadantin capsule containing a quick-release component and a slow-release component and a preparation method thereof. The furadantin capsule is characterized in that the mixture of 25 mg of furadantin and auxiliary material for quick-release medicine forms a quick-release part at one end in each capsule content, and the mixture of 81 mg of furadantin-hydrate and auxiliary material for slow release forms a slow-release part at the other end; and the slow-release part comprises the components in parts by weight: 81 mg of furadantin-hydrate, 14-25 mg of Carbomer 974P14, 13-15 mg of hydroxypropyl methylcellulose, 44-70 mg of povidone k30 and 5 mg of talc powder. The development of the furadantin slow-release capsule reduces drug administration times for patients, daily drug administration times are reduced to 2 times from 4-6 times, and the compliance of patients is obviously improved.
CN1981869B Compound non-carrier antibacterial eye drops containing practofren and its production An antibacterial eye medicine containing pranoprofen contains non-steroid antiphlogistic medicine, aminoglycoside-type antibacterial medicine, polyvinyl pyrrolidone, and pharmacologically acceptable carrier. Its preparing process is also disclosed.
DE102008031036A1 Use of 4-aminothiazolpyrimidine derivatives for the treatment of associated organ transplants Use of 4-aminothiazolpyrimidine derivatives (I) for the treatment of associated organ transplants, is claimed. Use of 4-aminothiazolpyrimidine derivatives of formula (I) for the treatment of associated organ transplants, is claimed. R 1>-R 5>not defined. [Image] - ACTIVITY : Immunosuppressive. - MECHANISM OF ACTION : None given.
EP1368002B1 Method for producing a floating tablet containing alfuzosine The invention relates to a method for producing a tablet containing alfuzosin, which is characterised in that it comprises the following steps: a given quantity of alfuzosin is prepared in accordance with the dosage for a given dissolution time; said quantity of active principle is homogeneously mixed with a quantity of carrier of between 50 and 99.9 % of the total weight, said carrier being chosen from among at least one compound from the family of cellulose derivatives and/or povidone derivatives and/or polyvinyl acetate derivatives; said mixture is compressed with a force in order to produce a homogeneous monolithic tablet that floats immediately in the gastric medium. The invention also covers the tablet obtained.
US7998922 Process for treating fibroses with biocompatible polymer A biocompatible polymer constituted by a sequence of identical or different components of the general formula (I): AaXxYy, in which A represents a monomer, X represents a carboxyl group fixed on a monomer A, Y represents a sulfate or sulfonate group fixed on a monomer A; a represents the number of monomers A, x represents the substitution rate of the set of monomers A by the groups X, y represents the substitution rate of the set of monomers A by the groups Y. The invention also pertains to the pharmaceutical or diagnostic compositions containing at least one polymer of general formula (I).
CN101945852A Azetidine derivatives, their preparation and their application in therapy The present invention provides the compounds conforming to the formula (I) in which: R represents a (C1-C6)alkyl or halo(C1-C6)alkyl group; R' represents a group NR4R5 or OR8; A and B, when present, represent independently of one another, one or two carbon atoms, these carbon atoms being substituted by one or more hydrogens or (C1-C6)alkyl groups; the (C1-C6)alkyl group or groups being optionally substituted; A+B represent two carbons at most; R1 represents a hydrogen atom or a (C1-C6)alkyl group; R2 and R3 represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group; the (C1-C6)alkyl group being optionally substituted; R4 and R5 represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group, or form, with the nitrogen atom which carries them, a heterocycle of the azetidine, pyrrolidine, piperidine, azepan, piperazine, homopiperazine, morpholine, thiomorpholine, thiomorpholine S-oxide or thiomorpholine S-dioxide type, this heterocycle being optionally substituted by a (C1-C6)alkyl group; R6 and R7 each represent a phenyl group, which is optionally substituted; Y represents a hydrogen atom, a halogen or a (C1-C6)alkyl group, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, (C1-C6)alkylS(O)p or cyano group; R8 is a hydrogen atom, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, an allyl group or a phenyl(C1-C6)alkyl group, the phenyl group being optionally substituted by 1 or 2 O-methyl groups; p represents an integer selected from 0, 1 and 2; in the form of the base or an addition salt with an acid or with a base. Preparation process and application in therapy.
CN1981746A Fluoxetine hydrochloride oral disintegrant tablets and their production An oral disintegrating tablet of fluoxetine hydrochloride features that the bitter taste of fluoxetine hydrochloride is masked by ion exchange resin. Its preparing process is also disclosed.
CA2163361C Therapeutic substituted guanidines The present invention provides therapeutically useful substituted guanidines of formula (I) and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
WO2013190510A3 NOVEL 2,3-DIHYDRO-1H-IMIDAZO{1,2-a}PYRIMIDIN-5-ONE and this1,2,3,4-TETRAHYDROPYRIMIDO{1,2-a}PYRIMIDIN-6-ONE DERIVATIVES COMPRISING A SUBSTITUTED MORPHOLINE, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF The invention relates to the novel products of formula (I) with p, q = 0, 1 or 2; R1 = phenyl, pyridyl; -(CH2) m -Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; -SO2 -Rb; -CO-Re; m = 1 or 2; Ra = aryl, heteroaryl, -CO-cycloalkyl, -CO-heterocycloalkyl, -CO-Rb, -C(Rb)=N-ORc, -CO 2 Rd, -CONRxRy; Rb = alkyl, aryl, heteroaryl; Rc = H, alkyl; Rd = alkyl, cycloalkyl; Re = alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry = H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3 = H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4 = H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
US20080131441 Methods of Using FOXP3 Levels to Predict the Outcome of Organs Undergoing Acute Rejection A method for assessing risk of losing a transplanted organ by a patient having an episode of acute rejection of the transplanted organ is described. The method includes obtaining from the patient a cell sample from the transplanted organ or peripheral blood, determining a level of FOXP3 in the cell sample, and correlating the level with the risk of loss of the transplanted organ, wherein, compared to a control level, a significantly greater level of FOXP3 in the cell sample from the transplanted organ or a significantly lower level of FOXP3 in the cell sample from the peripheral blood correlates with a decreased risk of loss of the transplanted organ.
CN101273995B Method for preparing magnetic particles modified by afi-tiazin dyes The invention relates to a preparation method of a phenothiazine dye modified magnetic particle. The preparation method comprises that the magnetic particle is suspended in a polar solvent, added with phenothiazine dye and auxiliary reagents, and after reaction for 6 to 12 hours at room temperature, a magnetic separation is carried out, the solids are washed by using 95 percent ethanol, thus obtaining the phenothiazine dye modified magnetic particle. The preparation method has the advantages of simple production and manufacture, low cost, non-toxic side effects and simple and convenient use.
CN101897697A Sugar-lowering drug composition and application The invention relates to a sugar-lowering drug composition and application thereof. The composition comprises 1) medicinal dosage of vildagliptin and 2) medicinal dosage of any one or combination of thiazolidinedione sugar-lowering drugs or medicinal salt thereof, sulfonylurea sugar-lowering drugs or medicinal salt thereof and biguanide sugar-lowering drugs or medicinal salt thereof. The invention relates to application of the sugar-lowering drug composition to preparing the drugs for treating and/or preventing diabetes or diabetic complications. The composition can effectively overcome the defect that type 2 diabetes can not be controlled by singly taking the commonly used sugar-lowering drugs or vildagliptin in the prior art and can reduce the diabetic complications.
WO2011091033A1 Modulation of neurogenesis by ppar agents The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system including by stimulating or increasing neurogenesis, neuroproliferation, and/or neurodifferentiation. The disclosure includes compositions and methods based on use of a peroxisome proliferator-activated receptor (PPAR) agent, optionally in combination with one or more neurogenic agents, to stimulate or increase a neurogenic response and/or to treat a nervous system disease or disorder.
US7351737 4-[(8-substituted)-6-chromanoyl]-and 4-[8-substituted)-chroman-6-YL-ethynyl]-benzoic and phenylacetic acids, their esters and salts having cytochrome P450RAI inhibitory activity Compounds of the formula where the variables are defined in the specification have cytochrome P450RAI-1 and P450RAI-2 inhibitory activity, and are suitable for treatment of mammals with conditions which are treatable with retinoids, or which are controlled by or responsive to the organism's native retinoic acid. Formulations containing the compounds of the invention can also be co-administered with retinoids and/or Vitamin A to enhance or prolong the effects of medications containing retinoids, Vitamin A, or of the organism's native retinoic acid.
WO2014093901A1 Triheptanoin for the treatment of glucose transporter 1 deficiency Provided are methods for treating GLUT1 and related brain energy deficiencies comprising administering odd-carbon fatty acid sources, e.g., C5 or C7 fatty acid sources, and related compositions.
EP1734962A2 Compositions and methods for modulating gated ion channels The present application relates to compositions which modulate the activity of gated ion channels. This provide an effect in the treatment of pain, inflammatory disorders and neurological disorders. Preferred compounds include quinine or quinidine derivatives with the hydroxyl at the nine position being esterified with an aliphatic carboxylic acid, optionally bearing an additional cycloalkyl ring on the chain. The gated ion channels modulated include homomultimeric and heteromultimeric gates.
US20100261766 Phenyl-Oxetanyl-Derivatives Novel organic compounds are described and claimed which may in particular be useful in the treatment of diseases being triggered by the (human) autoimmune system.
US20080161249 Use of Novel Antibacterial Compounds The present invention relates to the use of novel antibacterial compounds, and pharmaceutical compositions containing these compounds.
CN102579453A Compound preparation for treating gastric ulcer and preparation method of same The invention relates to the field of medicines, and discloses a compound preparation for treatment gastric ulcer. The compound preparation comprises active ingredients as follows: Irsogladine maleate raw material medicine and Omeprazole raw material medicine at a weight ratio of 1:15-25. The invention further particularly discloses an anti-ulcer compound preparation and a preparation method thereof. The anti-ulcer compound preparation contains 1-2% of Irsogladine maleate raw material medicine, 20-40% of Omeprazole raw material medicine, 5-10% of cross-linked polyvidone, 20-60% of lactose, 5-15% of cornstarch, 10-20% of microcrystalline cellulose, 1-3% of hydroxypropyl cellulose, 2-8% of magnesium stearate, 5-10% of sodium lauryl sulfate and 2-5% of disodium phosphate, and is prepared into tablets with 2-4% of white Opadry as the coating.
CN103070826A Quercetin skin lipidosome, lyophilized powder thereof and preparation method and application thereof The invention discloses a quercetin skin lipidosome and lyophilized powder thereof, belongs to the technical field of medicines, and aims to solve the problems that the quercetin is poor in solubility and difficult to apply, improve the penetration amount and the penetration rate of quercetin into a corneum and enhance the retention of a medicine in an epidermis and a dermis so as to play the efficacy better. Every 100 mL of lipidosome solution is prepared from the following substances: 0.01-0.1g of quercetin, 0.1-1.2g of amphiphilic lipid, 0.025-0.6g of cholesterol, 0.05-3g of surfactant, 0.001-0.5g of antioxidant and the balance of aqueous medium. The quercetin skin lipidosome and the lyophilized powder thereof are external preparations for a skin, and are applicable to oxidation resistance, inflammation resistance, ultraviolet radiation damage resistance, skin cancer resistance, and resistance to edema, red spots, pigmentation, inflammation and immune suppression which are caused by ultraviolet radiation.
CN103386136A Application of hydrophobic glucan in preparation of curcumin solubilizing agent and utilization method of hydrophobic glucan The invention discloses an application of hydrophobic glucan in the preparation of a curcumin solubilizing agent and a utilization method of the hydrophobic glucan. The hydrophobic glucan is prepared by reacting glucan with the molecular weight of 7.3*10<4>-16.8*10<4>g/mol with octenyl succinic anhydride for 1-5 hours under the conditions that the pH is 8-10, and the temperature is 15 to 55 DEG C. The influence of the degree of substitution, the molecular weight and the concentration of the hydrophobic glucan on the water solubility of the curcumin is also studied in the invention; the study shows that when the degree of substitution is 0.018, the concentration is 2.5mg/mL and the molecular weight is 16.8*10<4>g/mol, the water solubility of the curcumin is highest, and the solubility of the curcumin in water is increased from 11ng/mL to 11.7+/-1.7microgram/mL. The invention lays a foundation for the application of the curcumin in medicines and foods.
WO2008105498A1 Pharmaceutical composition for ameliorating inflammation induced by il-17 Disclosed are: an oligonucleotide useful for the inhibition of the production of IL-17, the inhibition of the proliferation of a CD4-positive T cell, the amelioration of an inflammation induced by IL-17 or the like; and an NR4A2 gene expression inhibitor, an IL-17 gene expression inhibitor, a CD4-positive T cell proliferation inhibitor or a pharmaceutical composition comprising the oligonucleotide as an active ingredient. Specifically disclosed is siRNA which can inhibit the expression of NR4A2 gene, such as an oligonucleotide having a nucleotide sequence depicted in any one of SEQ ID NOs:1 to 3. The siRNA is useful for the inhibition of the expression of NR4A2 gene, the inhibition of the expression of IL-17 gene, the inhibition of the proliferation of a CD4-positive T cell, the amelioration of an inflammation induced by IL-17 or the like.
CN102526069A External norgesterone acetate contraception preparation and preparation method thereof The invention relates to an external norgesterone acetate contraception preparation and a preparation method thereof. The external contraception preparation is characterized by being prepared from the following components in parts by weight: 0.005-0.05 part of norgesterone acetate, 1-100 parts of a medicament transport carrier, 3-40 parts of a transdermal absorption accelerant, 1-20 parts of fatty acid and 0.1-10 parts of a chelating agent. The external contraception preparation has a good contraception curative effect, and is a novel convenient and effective contraception preparation with high compliance.
CN101757637A Nasal pharmaceutical composition adopting cyclodextrin to include triamcinolone acetonide or 21-acetic ester thereof The invention relates to a nasal pharmaceutical composition adopting cyclodextrin to include triamcinolone acetonide or 21-acetic ester thereof. The nasal pharmaceutical composition comprises triamcinolone acetonide or the 21-acetic ester thereof and one or more pharmaceutically acceptable adjuvant materials, and is characterized in that the triamcinolone acetonide or the 21-acetic ester thereof as an active ingredient in the pharmaceutical composition is included by the cyclodextrin and/or a derivative thereof. The pharmaceutical composition is used for treating allergic rhinitis of humans or mammals.
CN102302549A Drug composition for treating cardiovascular and cerebrovascular diseases, preparation method and application thereof The invention discloses a dan-shen root and ligustrazine drug composition, a preparation method and an application thereof. According to the present invention, a plurality of experimental studies are adopted; the dan-shen root and the szechwan lovage rhizome are extracted through the supercritical fluid extraction method, wherein a weight ratio of the dan-shen root to the szechwan lovage rhizome is 5:1, the propanoid acid, the tanshinone IIA and the ligustrazine are adopted as index components; the experimental results show that: with adopting the preparation method provided by the present invention, the contents of the active ingredients can be significantly improved, the ligustrazine content is more than 100 mug/g; the results of the animal experiments show that: with adopting the preparation method provided by the invention, the significant pharmacologic action of the dan-shen root and ligustrazine drug composition is provided.
CN101716268B Powder for treating non-healing wound and bedsore The invention relates to external-use powder for treating a non-healing wound and bedsore, which is used for treating the non-healing wound, the bedsore and the like and prepared by a plurality of medicines. The powder comprises dragon blood, myrrh, olibanum, pearl, dragon bone and sugar. The invention fulfills the functions of promoting blood circulation, removing blood stasis, maturating, promoting wound healing, eliminating slough, promoting granulation and the like, treats various non-healing wounds, non healing after a surgery, the bedsore and the like, has the effect of treating both principal and secondary aspect of diseases, can achieve the purpose of difficult recurrence after healing, has the curative rate of 91.8 percent and the total effective rate above 99 percent in clinicalwork for many years, is well received by vast patients and wins high opinion.
WO2008075152A1 1- [4- (sulfonyl) -phenyl] -5- (benzyl) -ih-i, 2, 4-triazol derivatives as inhibitors of carbonic anhydrase for treating glaucoma or ocular hypertension The invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4 and RA through RE are as defined herein. The invention also relates to methods of treating glaucoma, ocular hypertension, age-related macular degeneration, diabetic macular edema, diabetic retinopathy, hypertensive retinopathy, retinal vasculopathies and intraocular pressure in mammals by administering the compounds of formula I, and to pharmaceutical compositions which contain the compounds of formula I for such treatments. The invention also relates to methods of preparing the compounds of formula (I).
US7060699 Aryl and heteroaryl diazabicycloalkanes, their preparation and use The present invention relates to novel aryl and heteroaryl diazabicycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
CN103127159A Application of aryl naphthalene type lignan in hepatitis C virus (HCV) therapy The invention relates to application of an aryl naphthalene type lignan in hepatitis C virus (HCV) therapy and belongs to the technical field of medicine, and discloses an aryl naphthalene type lignan (red fish eye glycoside B) which has the activity of HCV resistance and is extracted and prepared from a Guangxi special Zhuang medicine, namely, red fish eye Phyllanthus reticulatus. The application of the aryl naphthalene type lignan in the HCV therapy is characterized in that obvious inhibitory effect (p < 0.01) is supplied to replicon ribonucleic acid (RNA) of HCV within a concentration range of 125 microgrammes per rnl to 15625 microgrammes per rnl, and a concentration range of non-cytotoxic drugs is from 0 to 3125 microgrammes per rnl (p < 0.01). According to the application of the aryl naphthalene type lignan in the HCV therapy, the market prospect of aryl naphthalene type lignan (red fish eye glycoside B) in HCV resistance new drug research and development is wide.
WO2012000899A1 Semuloparin for use as an antithrombotic treatment in orthopaedic surgery with improved benefit-risk profile The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof as an antithrombotic treatment in patients undergoing major orthopaedic surgery, wherein said use involves an improved benefit-risk profile, compared to a standard antithrombotic treatment.
CN103193820A Nitrogen mustard phospholipid compound and preparation method thereof The invention discloses a nitrogen mustard phospholipid compound and a preparation method thereof. The compound expressed as the following formula in the specification and salts of pharmaceutically acceptable acids formed by the compounds are obtained through a chemical synthesis method, wherein R1 represents either -H or -CH3, R2 represents (ClCH2CH2)2NR3, R3 represents one or more of alkylene, aryl, aromatic alkylene and the like, and R1 and R2 can be identical or different; and the acids include inorganic acids such as hydrochloric acid, sulfuric acid, hydrobromic acid, phosphoric acid, carbonic acid and the like, as well as organic acids such as formic acid, acetic acid, citric acid, lactic acid, fumaric acid, tartaric acid, gluconic acid and the like. The compounds can be used as a liquid preparation, a solid preparation, a semisolid preparation, a sterilizing preparation and a sterile preparation.
WO2005099697A1 Use of phencynonate hydrochloride for treating or alleviating epilepsy The present invention relates to the novel use of phencynonate hydrochloride in medical field, in particular, the use of the compound for treating or alleviating epilepsy.
CN102988328A Method for preparing oral medicine for curing cancer, oral medicine for curing cancer and application thereof The invention discloses a method for preparing oral medicine for curing cancer. The oral medicine comprises two effective components of celecoxib and capecitabine. The preparing method includes that at least one component of the celecoxib and capecitabine is processed, simultaneously the processed celecoxib and capecitabine are filled in a same capsule, the dissolving of the celecoxib precedes that of the capecitabine, accordingly the effectiveness of the medicine for curing the cancer and synergy of medicine releasing are improved, and simultaneously the toxic and side effects of the medicine are greatly reduced. The invention further discloses the oral medicine prepared by the method and dosage proportion of crude drugs which form the oral medicine, by means of the oral medicine, tumor stem cells and tumor cells can be simultaneously killed, and the lifetime of a cancer patient is prolonged.
WO2006075152A1 4- (1h-indol-3-yl) -pyrimidin-2-ylamine derivates and their use in therapy The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof. The present invention seeks to provide further substituted heteroaryl-substituted pyrimidine derivatives. More specifically, the invention relates to compounds that have broad therapeutic applications in the treatment of a number of different diseases and/or that are capable of inhibiting one or more protein kinases.
CN102040516A Resveratrol derivative and medical application thereof The invention relates to a resveratrol derivative and a medical application thereof, and in particular discloses a compound in a formula I as shown in the specification or pharmaceutically acceptable salt, ester, solvate and stereoisomer thereof, wherein R1, R2 and R3 are respectively independently selected from hydrogen atom, C1-C3 alkyl groups, or a substituent group in a formula i as shown in the specification, at least one of R1, R2 and R3 is selected from the C1-C3 alkyl groups, and simultaneously at least one of R1, R2 and R3 is selected from the substituent group in the formula i; R is selected from hydrogen atom, substituted or unsubstituted C1-C5 alkyl groups, substituted or unsubstituted C3-C6 naphthenic groups, benzyl groups or phenyl groups; and R4 and R5 are respectively independently selected from hydrogen atom, substituted or unsubstituted C1-C5 alkyl groups, or substituted or unsubstituted C3-C6 naphthenic groups. The invention also discloses a pharmaceutical composition containing the compound in the formula I, and the application of the compound in the formula I in preparing medicines for treating and/or preventing cardiovascular and cerebrovascular diseases. The compound in the formula I provided by the invention can be effectively used for treating and/or preventing the cardiovascular and cerebrovascular diseases such as hyperlipidaemia.
CN102844032A Compound for treatment of respiratory condition or disease The present invention relates to the treatment, alleviation, prevention or reduction of symptoms or exacerbations of asthma or chronic obstructive pulmonary disease (COPD), of which reduced lung function is typically symptomatic.
CN101049356A Pharmaceutical composition of containing puerarin and leaves of hawthorn A medical composition in the form of injection or orally taken solid or liquid for treating coronary heart disease, angina pectoris, hypertension, cerebrovascular disease, hemicrania, diabetes, etc is proportionally prepared from kakonein and hawthorn leaf flavone.
WO2011010682A1 Sterol derivative Disclosed is a sterol derivative, which has an effect of promoting the proliferation of nerve stem cells, or a pharmaceutically acceptable salt of the same. Specifically disclosed is a sterol derivative represented by general formula (I) [wherein Y represents an optionally substituted lower alkyl, etc.; Xa and Xb are the same or different and represent a bond, etc.; R1, R2, R3, R4, R7 and R8 are the same or different and represent a hydrogen atom, etc.; R5 and R6 are the same or different and represent a hydrogen atom, etc.; R9 represents a hydrogen atom, etc.; R10 and R11 together form a bond, etc.; and R12 represents a hydrogen atom, etc.], a pharmaceutically acceptable salt of the same, or the like.
EP2345656A1 Helicobacter pylori bacterium proliferation inhibitor The present invention herein provides a proliferation inhibitor of H. pylori bacteria comprising a compound that can specifically inhibit the proliferation of H. pylori bacteria, which does not generate bacterium resistant, can be eaten, drunken or administrated safely for a long period of time, can be simply mass-manufactured and can be used for foods and beverages or pharmaceutical preparation. The proliferation inhibitor of H. pylori bacteria comprises an N-acetylglucosaminyl beta-linked monosaccharide derivative represented by the following chemical formula (1): GlcNAc1-beta-O-Y (1) wherein Y is an alkyl group, an alkoxyl group, an alkenyl group, an alkynyl group, an aralkyl group, an aryl group, a heteroaryl group, a carboxyl group or an alkoxycarbonyl group.
CN102584809A Amion thiazolidone compound, method for preparing same and application thereof in preparing antitumor drugs The invention provides an amion thiazolidone compound, as shown in a formula I, wherein A1 is aryl or ceteroary; A2 is benzene ring or substituted benzene ring, double benzene nucleus or substituted double benzene nucleus, pyridine ring (including 2-, 3-, 4-pyridine) or substituted pyridine ring; and R1, R2, R3, R4, R5 and R6 are respectively H, halogen, hydroxy, cyan, amino or nitro or C1-C6 alkyl or C1-C6 alkoxy and the like; and R7 and R8 are respectively H, C1-C6 alkyl or C3-C6 naphthene base. The compound in the formula I comprises hydrate of the compound, solvate, stereoisomer, N-oxide, salt and crystalline forms which exist in various forms. Bioactivity tests show that: the compound in the formula I can restrain the activities of polo-like kinase 1 (PLK1) inside and outside the human body, and can be used for preparing antitumor drugs. The invention further provides a method for preparing the compound in the formula I.
CN201076616Y Female health care suppository pill The utility model relates to a healthy suppository pill for female, wherein the main body takes a small-sized ball shape which comprises a ball body and a ball tail, the ball body comprises an intermediate pill body and an external capsule, the ball tail comprises a tying portion and an outer guiding lead, the intermediate pill body contains pure natural medicinal material such as phellodendron bark, safflower, sophora flavescens ait, cnidium monnieri, pseudolarix, Chinese pulsatilla root, broom cypress fruit, dragon blood, dried alum, Chinese dittany bark and the like, and auxiliary material such as borax and borneol to process pills with honey, the pill has the function of diminishing inflammation, activating blood circulation, removing itch, deodorizing and removing moisture, the external capsule is made of sterilized gauze, and the outer guiding lead can be fixed on the tying portion of the external capsule. When in use, the ball body is positioned in the deep place of the vagina, the outer end of the outer guiding lead is positioned on the vaginal orifice, after 8 hours, a turbid ball body whose inner portion is adsorbed with female virus and the outer surface is adhered with silting substance is taken out. The utility model can be used according to the treatment course or use after each catamenia is finished according to the practical needs, good effect of physical therapy and healthcare can be achieved after insist on using, and the utility model is an ideal healthcare article which is particularly applied to grow-up females.
WO2007146087A3 SUBSTITUTED PYRAZOLO [1,5-α] PYRIDINE COMPOUNDS AND THEIR METHODS OF USE The present invention is directed to substituted pyrazolo[l,5-α]pyridines and related methods for their synthesis and use.
EP1109908B1 Methods for determining compounds for modulating the body weight Six genes whose expression is induced by leptin are disclosed (LIG46; LIG56; Tgtp, encoding a T cell-specific GTP-binding protein; LRG-47, encoding an interferon (IFN) inducible protein; RC10-II, encoding a subunit of a 20S brain proteasome; and Stra13, encoding a retinoic acid inducible protein). These six leptin-inducible genes and the proteins they encode represent targets for the development of therapeutic agents for use in modulating body weight. For example, agents that alter the expression or activity of one or more of the leptin-induced proteins can be used to modulate body weight. Such agents can be identified using cellular, in vitro, or in vivo assays which monitor the expression or activity of one or more of the six leptin-induced proteins. Potentially useful therapeutic agents can also be identified through the use of assays designed to identify agents that bind to one of the leptin-induced proteins. The leptin-induced genes of the invention and the proteins they encode may themselves be useful therapeutically and diagnostically.
CN103638005A Application of Hippolachnin A in medicine for treatment or prevention of dental ulcer The invention relates to application of Hippolachnin A in medicine for treatment or prevention of dental ulcer, which is disclosed for the first time; as the skeleton type belongs to a brand new skeleton type, and the dental ulcer treatment activity is high, the Hippolachnin A has outstanding substantive features and has an obvious progress in the treatment of dental ulcer.
CN102579369A Sodium butyrate enteric sustained release preparation and preparation method thereof The invention discloses a sodium butyrate enteric sustained release preparation and a preparation method thereof. The method comprises the following steps of: synthesizing sodium butyrate by a synthetic process, performing clathration on a synthesized sodium butyrate liquid in the liquid state, spraying and granulating to obtain the sodium butyrate enteric sustained release preparation. Accordingto the method, production links and production cost are reduced, the influence of the production process on environment is reduced, and the volatile smell and hygroscopicity of the product are reduced; and the prepared sodium butyrate enteric sustained release preparation is white spherical particles, and the particle size is 200 to 500 micrometers. The sodium butyrate enteric sustained release preparation is high in stability and humidity resistance and can be released in intestinal tracts slowly, so that the bioavailability of the product is improved.
CN101058810A Amphioxus uncoupling protein gene and application thereof The invention relates to an amphioxus uncoupling protein (UCP) molecule clone and the functional research in the biotechnology field. The invention clones uncoupling protein (UCP) gene from amphioxus firstly with degeneracy primer and 3', 5'-RACE, which expresses muscle, intestinal canal and gill widely. Heightening UCP expression on the third day with dealing in low temperature indicates UCP engaging in body heat regulation in low temperature; Reducing UCP expression with hungry for fourteen days indicates that UCP engages in energy metabolism regulation. UCP is related to many diseases as diabetes, cardiovascular disease, tumour and so on, so UCP can be produced medicines treating these diseases.
CN102973567A Beta-lactamase antibiotic drug composition The present invention provides a beta-lactamase antibiotic drug composition, which comprises cefuroxime or salt powder thereof, and sulbactam or salt powder thereof, wherein a particle size of the cefuroxime or the salt powder thereof is 80-150 mesh. According to the drug composition, a good content uniformity is provided, drug quality is ensured, and important significances are provided for medication safety and effectiveness.
CN101130539B Indole-substituteing imidazoline-2-ketones derivant, preparing method and uses of the same The invention discloses an indole to replace imidazoline-2-ketones derivant, which is characterized by the following: choosing natural product Combretastatin A-4 as lead compound; replacing ethene chain with imidazoline-2-ketone five-membered hetero ring; replacing benzene ring in CA-4 with indole ring; getting a series of imidazoline ketones derivant. This invention can be used to prepare antitumor agent, which possesses the function to inhibit tumor cell propagation and simple preparing method.
US20100233152 Use of HMGB proteins and nucleic acids that code therefor The invention relates to the use of HMGB and/or a nucleic acid that codes therefor and/or an interaction partner of HMGB that is in particular natural and/or a nucleic acid that codes therefor as a target molecule for the development and/or production of a medicament for the treatment and/or prevention of diseases of the endometrium and/or for the development and/or production of a diagnostic agent for diagnosing diseases of the endometrium.
EP1671652A1 Use of chitosan for the treatment of pruritus Use of chitosan (I) and/or its derivate for the production of topic preparation against itching. An independent claim is also included for a topic preparation for the treatment of itching, comprising chitosan and hydroxy acid (0.01-5 wt. %). - ACTIVITY : Antipruritic; Dermatological; Antiinflammatory. - MECHANISM OF ACTION : None given.
CN100574758C Compound for treating ischemic related disease The present invention relates to methods of treating ischemia-related conditions by administering to a patient in need of such methods certain thiosemicarbazone compounds. Preferred embodiments of the present invention relates to methods of treating specific ischemia-related conditions, including but not limited to Alzheimer's disease, Parkinson's disease, Coronary artery bypass graft surgery, Global cerebral ischemia due to cardiac arrest, focal cerebral infarction, cerebral hemorrhage, hemorrhage infarction, hypertensive hemorrhage. hemorrhage due to rupture of intracranial vascular abnormalities, subarachnoid hemorrhage due to rupture of intracranial arterial aneurysms, hypertensive encephalopathy, carotid stenosis or occlusion leading to cerebral ischemia, cardiogenic thromboembolism, spinal stroke and spinal cord injury, diseases of cerebral blood vessels: e.g., atherosclerosis, vasculitis, Macular degeneration, myocardial infarction, cardiac ischemia and superaventicular tachyarrhytmia.
WO2007009354A1 Pyrrolidine derivative intermediates,preparation and usage thereof The present invention discloses a kind of compounds of general formula (I), in which PNZ is p-nitrobenzyl-oxycarbonyl, R is Ac or H, as well as the preparation method of the compounds and their usage as intermediate in the preparation of novel 1β-methylcarbapenem antibiotic-doripenem and the preparation method of doripenem. The pyrrolidine derivative intermediates do not have Boc-protecting group and avoid side reaction caused by acidolysis , so the present method is simple and it is convenient for purifying the product and is cost-efficient.
WO2011006960A1 Spiro amino compounds suitable for the treatment of inter alia sleep disorders and drug addiction The invention concerns a spiro-amino compound of Formula (Vl) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O e N, such ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, halogen, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridil, pyrimidil, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.
CA2440172C Itraconazole solution A solution for oral administration comprising itraconazole, an alcoholic solvent, and an acid.
CN103230366A Novel slow-release breast perfusion agent for preventing cow subclinical mastitis and preparation method thereof The invention provides a novel slow-release breast perfusion agent for preventing cow subclinical mastitis and a preparation method thereof. 100g of the novel slow-release breast perfusion agent comprises 1 to 5g of cephapirin benzathine, 0.5 to 8g of polyethylene glycol-400, Tween materials or propylene glycol, 0.5 to 8g of fatty alcohol-polyoxyethylene ether, cyclomethylene glyceryl ether, glyceryl triacetate or poloxamer, 0.02 to 0.05g of vitamin E, 0.05 to 0.1g of benzyl alcohol, and the balance soybean oil for injection, liquid paraffin or median-chain triglyceride. The invention also provides a preparation method of the novel slow-release breast perfusion agent. The novel slow-release breast perfusion agent is suspended colloid, can be released slowly, has low administration frequency, can prevent cow subclinical mastitis in a mild shortage stage, and does not produce residues in milk in a lactation stage. Compared with foreign like products, the suspended colloid has better stability.
CN101269007A Dosage form containing levorotation gossypol as active component The invention relates to a pharmaceutical preparation taking levorotatory gossypol as active ingredient, in particular to a compound preparation which contains the medicine such as levorotatory gossypol, potassium chloride, vitamin B1 and vitamin B6, etc. and is used for curing gynecological disease. The compound preparation comprises an oral solid preparation and an injection.
CN103462995A Application of Neonectrolide A in preparing a medicament for treating hemorrhagic fever with renal syndrome The invention discloses novel application of Neonectrolide A in preparing a medicament for treating hemorrhagic fever with renal syndrome. In-vitro and in-vivo inhibition experiment researches indicate that Neonectrolide A has low toxicity to cells, can be directly used for killing viruses of hemorrhagic fever with renal syndrome, and can remarkably inhibit multiplication of the viruses; a hamster infected by the viruses can be remarkably protected, the attack time can be postponed, the course of disease can be prolonged, and the death rate can be reduced, so that Neonectrolide A is an effective and safe medicament for treating hemorrhagic fever with renal syndrome.
WO2010047295A1 Medicine for preventing or treating pain related to herpes zoster Provided is a pharmaceutical composition for preventing or treating pain related to herpes zoster. A N-{2-[(4-substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxide compound that is useful as an anti-varicella-zoster virus (VZV) agent has an unexpected effect in the prevention of irreversible neurodegeneration accompanying herpes virus infections, and is thus also useful as an agent for preventing or treating pain related to herpes zoster.
US20120077839 Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-ol compounds and methods relating thereto Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds are disclosed that are inhibitors of the vesicular monoamine transporter 2 (VMAT2). The compounds of this invention have the structure: wherein R1 is as defined herein, including stereoisomers and pharmaceutically acceptable salts and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use in a subject in need thereof.
US20100113535 Treatment of presbyopia with alpha- picolinic acid and its analogs Compositions and methods for inhibiting the growth of lens epithelial cells are provided. The compositions provided include a chelating agent in an amount sufficient for inhibiting the growth of lens epithelial cells. The compositions and methods provided may also be used for the treatment of disorders of the eye, especially in the treatment of presbyopia.
CN102038677A Brominated dihydroartemisinin compound double-releasing preparation The invention discloses a novel brominated dihydroartemisinin compound double-releasing preparation and preparing components thereof. The preparation is maximally characterized by comprising the steps: preparing a compound preparation from the brominated dihydroartemisinin and the ferrous sulfate, dissolving and fast releasing a ferrous sulfate micro ball in the stomach in the same preparation, and dissolving and fast releasing a brominated dihydroartemisinin micro ball in the intestine, thereby solving the problem that the brominated dihydroartemisinin and the compounded agent ferrous sulfate can be taken simultaneously but can be dissolved in the stomach simultaneously. The technology of the novel brominated dihydroartemisinin compound double-releasing preparation is simple, is easy to operate, is suitable for the industrialized production, and leads a product to be higher in quality stability, better in anticancer effect, and lower in side effect.
WO2012175702A1 Rimfampicin analogue useful for infection imaging The present invention provides radiolabelled RIF derivatives that are suitable for in vivo imaging of bacterial infection. The in vivo imaging agent of the invention is preferably provided as a radiopharmaceutical composition, which forms a further aspect of the invention. Also provided by the present invention is a precursor compound useful in the preparation of the in vivo imaging agent of the invention, a method for the preparation of the in vivo imaging agent of the invention comprising reaction of the precursor compound with a suitable source of the desired radiolabel, and methods for the use of the in vivo imaging compound.
US20050107616 Alpha-ketoamide derivatives as cathepsin k inhibitors Biaryl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such biaryl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.
WO2006123183A3 Sulphone derivatives for treatment of cancer Coumpounds of Formula (I) are disclosed for treatment of cancer.
EP1307226B1 Vitronectin receptor antagonist pharmaceuticals The present invention describes novel kits and compositions comprising compounds of the formula (I): (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer in combination therapy in a patient. The present invention provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.
WO2009010529A1 Synergistic combinations of vr-1 antagonists and cox-2 inhibitors A synergistic combination of a vanilloid receptor VR-1 antagonist and an NSAID or a pharmaceutically acceptable salt or solvate of either or both compounds thereof.
CN101953773A Lamivudine liposome solid preparation The invention discloses a lamivudine liposome solid preparation and further discloses application thereof in treating chronic hepatitis B. The liposome solid preparation comprises lamivudine, dipalmityl phosphatidyl glycerol, sodium deoxycholate and cholesterol, can be prepared into tablets, dispersible tablets, capsules and the like, has the advantages of high entrapment rate, good stability, improved dissolving rate and the like, and shows favorable safety and drug resistance, better antiviral effects, and lower drug resistant rate and virus bouncing rate on treating the chronic hepatitis B.
US6855686 Also administering to the subject an effective amount of an mda-7 protein. This invention provides a method for reversing the cancerous phenotype of a cancer cell by introducing a nucleic acid having the melanoma differentiation associated gene (mda-7) into the cell under conditions that permit the expression of the gene so as to thereby reverse the cancerous phenotype of the cell. This invention also provides a method for reversing the cancerous phenotype of a cancer cell by introducing the gene product of the above-described gene into the cancerous cell so as to thereby reverse the cancerous phenotype of the cell. This invention also provides a pharmaceutical composition having the melanoma differentiation associated gene (mda-7) or the gene product of the melanoma differentiation associated gene (mda-7) effective to reverse the cancerous phenotype of a cancer cell and a pharmaceutically acceptable carrier.
US7390890 1,4-Dideoxy-1-C-(4-hydroxypyrrolo[3,2-d]pyrimidin-7-yl)-1,4-imino-D-ribitol derivatives or salts; parasite purine nucleoside, -hydrolase, -phosphorylase and/or phosphoribosyl transferase inhibitors; antiprotozoa, anticarcinogenic, antiinflammatory, and immunosuppressant agents; autoimmune diseases The present invention provides compounds having the formula: wherein A is CH or N; B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H, halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and X and Y are independently selected from H, OH or halogen except that when one of X and Y is hydroxy or halogen, the other is hydrogen; and Z is OH or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof; and compounds having the formula: wherein A, X, Y, Z and R are defined for compounds of formula (I) where first shown above; E is chosen from CO2H or a corresponding salt form, CO2R, CN, CONH2, CONHR or CONR2; and G is chosen from NH2, NHCOR, NHCONHR or NHCSNHR; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof. The present invention also provides the use of the above compounds as pharmaceuticals, pharmaceutical compositions containing the compounds and processes for preparing the compounds.
CN101328476A Nucleic acid molecule NRN1SR32 and use thereof in anti-cancer medicine preparation The invention belongs to the biomedical field and relates to NRN1SR32 and an application of the NRN1SR32 in the preparation of an antitumor drug. The tumor threatens the health of people. The invention provides the nucleotide molecule NRN1SR32 used for preparing the antitumor drug, and the sequence comprises 5'-TCTCTTGAACCATTTGCGACCGCAGACCA-3' or 5'-UCUCUUGAACCAUUUGCGACCGCAGACCA-3'. Compared with nude mice without the NRN1SR32 in the same culture condition, the nude mice containing the NRN1SR32 has a tumor body prevented from growing evidently; moreover, the phenomenon is more evident as time goes on. The product provides a novel way and method for treating and relieving the tumor.
CN103463123A Method for extracting effective constituents from maca The invention provides a method for extracting effective constituents from maca. The method includes the following steps that fresh or dry maca roots are taken as raw materials, the maca roots are washed, impurities are removed, an ethyl alcohol-water solution is used as homogenate liquid, the maca roots are homogenized, crushed and extracted, so that a homogenate extracting solution is obtained, filtering is conducted, filtering residues are mixed with an extraction solvent, negative pressure cavitation solid-liquid mixing cyclone extraction is conducted to obtain the extracting solution, the extraction solutions are combined and concentrated, a concentrated solution and a low-level solvent are mixed, then negative pressure cavitation liquid-liquid extraction is conducted, an extracting liquor is obtained, an extract is obtained after concentration, ethyl alcohol is added for redissolving, and thus a solution 1 is obtained; the extracted maca filtering residues are extracted again through hot water, an extracting solution is obtained after filtering, and a solution 2 is obtained after concentration; the solution 1 and the solution 2 are combined and dried, and extractives of the effective constituents of the maca are obtained. The method for extracting the effective constituents from the maca has the advantages that the technological process is simple, the production cycle is short, the effective constituents can be efficiently extracted, products can maintain the original flavor of the maca, used equipment is conventional equipment, production cost is low, and industrial production is easy to achieve.
CN101757308A Healthcare medicine for preventing and treating poultry respiratory symptoms The invention relates to a healthcare medicine for preventing and treating poultry respiratory symptoms, which comprises the following raw materials in parts by weight: 20-25 parts of Chinese ephedra, 55-58 parts of semen armeniacae amarae, 88-92 parts of gypsum, 58-62 parts of licorice, 78-80g of isatis root, 75-78 parts of radix sophorae subprostratae, 48-50 parts of radix platycodi, 48-52 parts of fructus forsythiae, 60-62 parts of radix scutellariae, 72-75 parts of rhizoma belamcandae and 78-80 parts of cordate houttuynia. Clinical trials prove that the healthcare medicine has obvious curative effect on poultry symptoms caused by various factors such as acute respiratory inflammation, chronic respiratory inflammation, dyspnea, cough, stridor and the like, thus being a novel, efficient, residue-free, safe and low-price healthcare medicine for preventing and treating poultry respiratory symptoms.
CA2087883C Beta-alethine use in cell culture and therapy .beta.-alethine is employed in the differentiation, phenotypic expression, and vitalization of cells, for both in vivo and in vitro applications. Particular applications include the use of .beta.-alethine in the treatment of immune disorders and diseases, especially neoplasia, and in the promotion of cell cultures.
US20070259945 Method for treating pain The present invention provides pharmaceutical compositions useful in a method for treating neuropathic pain, said method comprising administration of a pain-ameliorating effective amount of the compound according to formula I wherein X may be Y may be wherein R is H or (CH2)mH, alternatively the bond between X and Y may be a double or triple bond, e.g. X═Y or X≡Y; wherein n is an integer of from 1 to 10, m is an integer of from 1 to 4 and the total carbon atoms in the alkenyl amide chain is from about 11 to about 20 as an active ingredient together with one or more pharmaceutically-acceptable additives, excipients or diluents.
EP2535047A1 Nutritional composition, food supplement comprising said nutritional composition and kit comprising said food supplement The present invention relates to a nutritional composition allowing yielding benefits to the urinary tract, as well as to a food supplement containing said composition. According to the invention, in said nutritional composition D-mannose is associated with a pH stabiliser, which is arranged to maintain the pH in a range of values from about 6.0 to about 6.5 and which allows optimising the effectiveness of D-mannose. The present invention also relates to a kit of food supplements comprising a first food supplement containing the nutritional composition mentioned above and a second food supplement containing a second nutritional composition comprising D-mannose.
WO2011034828A1 Substituted para-biphenyloxymethyl dihydro oxazolopyrimidinones, preparation and use thereof The present invention relates to a series of substituted para-biphenyloxymethyl dihydro oxazolopyrimidinones of formula (I) as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
CN102872125A Application of Houttuynoid C in medicament for treating cervical cancer The invention discloses application of Houttuynoid C in preparing a medicament for treating human cervical cancer, and belongs to the technical field of new use of medicaments. Houttuynoid C is found to have an obvious inbibitional effect on the growth of human cervical cancer cell lines HeLa, HeLa229, HCE1 and CaSKi through MTT (Methyl Thiazolyl Ternzolinm) anticancer activity evaluation in vitro. Therefore, Houttuynoid C can be used for preparing the anti-cervical cancer medicament and has excellent prospects in development and application. The use of Houttuynoid C in preparing the medicament for treating the human cervical cancer involved in the invention is disclosed for the first time; the framework type of Houttuynoid C is a brand new framework type and Houttuynoid C has an unexpectedly high inhibition activity for human cervical cancer cells.
WO2008150197A1 Biologically active additive for preventing and treating asthma and diseases of the upper air passages and a method for the production thereof The invention relates to medicine and the food industry. The inventive biologically active additive for preventing and treating asthma and diseases of the upper air passages contains a solution of a dry extract of Boswellia serrata, the content of boswellic acids in which in terms of β-boswellic acid is equal to or greater than 80%, in a wheat-germ oil and is encapsulated, together with a pharmaceutically acceptable selenium source, into an envelop containing glycerin, gelatin, a pharmaceutically acceptable zinc source and a dry chicory extract. A method for producing the additive, consists in successively solving the pharmaceutically acceptable zinc source, the dry chicory extract, gelatin and glycerin in cleaned water and in agitating said mixture, in forming the envelop from the produced paste, in filling said envelop with a solution to be encapsulated which is produced by mixing the wheat-germ oil and the pharmaceutically acceptable selenium source and by subsequently gradually adding the dry extract of Boswellia serrata, the content of boswellic acids in which in terms of β-boswellic acid is equal to or greater than 80%, until it is totally diluted, in holding the thus produced capsules at a temperature of 5-10°C and in drying said capsules. The produced biologically active additive is highly efficient.
EP2162458A1 Protein kinase-binding nucleosides and associated methods Therapeutically active nucleosides and associated methods are provided. In one aspect, a nucleoside molecule having a general structural similar to ATP. Such nucleosides have a structure that allows binding to, and subsequent regulation of, protein kinase molecules. As such, the nucleosides of the present invention may be capable of treating a variety of kinase-related medical disorders.
US20090105284 Aminocyclohexanes as Dipeptidyl Peptidase-IV for the Treatment or Prevention of Diabetes The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
WO2009095253A1 6-halo-pyrazolo[1, 5-a]pyridines, a process for their preparation and their use as metabotropic glutamate receptor (mglur) modulators The invention relates to 6-halo-pyrazolo[1, 5-a] pyridines of formula (I) as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.
US20130101653 Methods and materials for reducing the risk of infections This document relates to methods and materials for reducing the risk of infection after a shoulder surgery or medical procedure. For example, this document relates to methods and materials for using a topical composition containing clindamycin or erythromycin to reduce the risk of or to prevent infection associated with shoulder surgeries or medical procedures.
WO2012159237A1 Quick release-sustained release composition of compound methoxyphenamine Quick release-sustained release composition containing methoxyphenamine or hydrochloride thereof, narcotine, aminophylline and chlorphenamine maleate is disclosed by the present invention. The quick release part has 1-70% effective components and the sustained release part has 30-99% effective components,and the release time is 8-24 hours. The preparations of the quick release-sustained composition includes a quick release-sustained release tablet, a quick release-sustained release capsule or a quick release-sustained release suspension.
WO2005117867A3 Monocyclic heterocycles as kinase inhibitors The present invention is directed to compounds having the formula [I + II] and methods for using them for the treatment of cancer.
CN102614194A Externally applied medicine for treating skin disease and application thereof The invention discloses an externally applied medicine for treating skin disease and application thereof. The medicine consists of an active ingredient and pharmaceutically acceptable auxiliary materials, wherein the active ingredient is a mixture of diflorasone and adapalene, or a mixture of diflorasone and acitretin, or a mixture of diflorasone, adapalene and acitretin. The invention overcomes the defects of poor treatment effect and high side effect of single medication, and the diflorasone and the adapalene or/and the acitretin are compounded to form the compound externally applied medicine. The preparation can be prepared into externally applied formulations in different forms; and due to synergic and complementary effects of medicines, the compound externally applied medicine has high treatment effect, lightens the adverse reaction of the patient in clinical application, has an obvious treatment effect on skin disease, and is easily accepted by the patient.
US20110251134 Combination of (a) a dna toposomerase inhibitor and (b) an iap inhibitor The invention relates to a pharmaceutical combination which comprises (a) a DNA topoisomerase inhibitor compound and (b) a compound that inhibits the caspase-9 inhibiting properties of an inhibitor of apoptosis protein (IAP) for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
US20090093639 Prodrugs of carbamate inhibitors of IMPDH The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds and compositions of this invention.
CN101262855A Method of treatment or prevention of age-related macular degeneration A method of treatment and/or prevention of age-related macular degeneration (AMD) wherein, in a first step, the need for treatment or susceptibility to AMD is determined for an individual and, in a second step, a medication comprising lutein and/or zeaxanthin and/or certain antioxidants (or a mixture thereof) is tailored to that individual. The invention also provides a method of determining a substance to be administered to an individual, which individual may be susceptible of having age-related macular degeneration (or an age-related macular degeneration-related disorder) comprising: a) determining the susceptibility of the individual to age-related macular degeneration (usually genetically, by detection of an SNP); and b) on the basis of the determination in a), identifying a substance capable of preventing or treating age-related macular degeneration in that individual. The method may additionally comprise providing (such as administering or communicating) the substance (or its identity) to the individual.
US7316818 Liposome drug delivery of polycyclic, aromatic, antioxidant or anti-inflammatory compounds This invention comprises pharmaceutical compositions for administering a polycyclic, aromatic, antioxidant or anti-inflammatory compound to an animal. Particularly provided are proliposomal compositions that are advantageously used to deliver polycyclic, aromatic, antioxidant or anti-inflammatory compounds to the gastrointestinal tract after oral administration.
US20050261502 2-Amino-4-(1,3-benzodioxol-5-yl)-6-benzyloxy-3,5-pyridinedicarbonitrile, acting as adenosine-receptor-selective ligands, for the prophylaxis and/or treatment of cardiovascular disorders The use of compounds of formula (I) as medicaments, novel compounds of formula (I) and a method for production thereof are disclosed. Compounds of formula (I) are effective as adenosine receptor ligands.
CN103156903A Externally-used medicament for treating measles pneumonia The invention relates to an externally-used medicament for treating measles. The measles is an acute infectious disease caused by measles zoster virus infection, and strong in infectivity, and is relatively common in winter and spring, and often epidemic. The medicament is prepared by grinding morning glory seeds, alum, vinegar and dried powder into fine powder, made into paste, and applied to Yongquan acupoints at both sides. The medicament is capable of dispelling wind and relieving superficies, clearing heat and detoxifying, soothing the liver and resolving depression, promote eruption and eliminate sore and the like, and has advantages of simple external use, convenient usage and good curative effects.
WO2006045820A1 Pharmaceutical compositions based on nk2 antagonists for pediatric use Pharmaceutical compositions containing NK2 antagonists are described, useful for the treatment of infantile colics.
US20090005435 Novel Compounds, Pharmaceutical Compositions Containing Same, and Methods of Use for Same A pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula (II), wherein R1 and R2, the same or different from each other, are H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —CH2CORS, —CH2C(O)NRS, —C(O)R5, or —CH2OR5, and can optionally contain halogen atoms, where R5 is a C1-C12 alkyl group. R3 and R4, the same or different from each other, are H, C1-C20 alkyl cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl.
EP2356986A1 Composition for treatment of metabolic syndrome The invention relates to a composition comprising a combination of a dimer-gallate and a trimer, useful as a medicament for the treatment and/or prevention of metabolic syndrome or of a pathology associated therewith, wherein the dimer-gallate is a procyanidin B-gallate, differing from B2-gallate, and the trimer is a procyanidin C. It also relates to the use of said composition in the preparation of a food, a food additive or a dietary supplement.
US8252909 Synthetic C-glycolipid and its use for treating cancer, infectious diseases, and autoimmune diseases The invention is directed to compounds of formula (I) wherein X is O or NH; R′ is a hydrocarbon chain; R3 and R4 are hydrogen, OH or a monosaccharide; R5 is hydrogen or a monosaccharide; Q′ is optionally present and may be a C1-10 hydrocarbon; X′ is optionally present and may be O, S or NR8; and Q3 may be a hydrocarbon or hydrogen. The invention is also directed to the use of the compounds for treating cancer, infectious diseases and autoimmune diseases. The invention is also directed to syntheses of the compounds of formula (I).
US20120100208 Stable pharmaceutical composition and methods of using same The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases.
CN101496805A Application of 4-acetyl diazene quinoline derivatives in preparing anti-tumor medicament The invention belongs to the field of genetic engineering and chemistry, and relates to application of 4-acetyl diazenyl quinoline in preparing an anti-tumor medicine. Searching for a novel anti-tumor medicine with low side effects is a hot spot in the field of biological medicine. The invention provides application of a micromolecular compound 1-[2-(3-phenelyl)quinoline-4-group]-2-{[4-methoxyl-3-(morpholinomethyl)phenyl]diazene}ethyl ketone in preparing the anti-tumor medicine. The compound can obviously inhibit the proliferation of tumor cells, is designed aiming at the CYPJ protein structure of cell target spots, and particularly has obvious effect on tumor cells with high-expression CYPJ proteins. Therefore, the micromolecular compound is developed by being taken as a novel anti-tumor medicine, and has good anti-tumor effect and good specificity.
CN103446111A Applications of Sarcaboside B in medicament against influenza A virus The invention discloses applications of Sarcaboside B in preparing a medicament against influenza A virus. Experiments prove that the Sarcaboside B has a remarkable inhibition effect on the influenza A virus, thus indicating that the Sarcaboside B has a potential application value in the field of treating influenza A virus infectious disease. The applications of the Sarcaboside B in preparing the medicament against influenza A virus are disclosed for the first time. As a skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpectedly strong influenza virus inhibition activity, and the possibility of giving any inspiration by other compounds does not exist. The Sarcaboside B has significantly substantive characteristics, as well as obviously prominent progress in the prevention and treatment of the influenza virus infection.
EP1779863A1 Use of TGF-Beta and growth factors in the treatment and prevention of diseases of the intestinal mucosa The invention pertains to the use of transforming growth factor β (TGF-β) in the preparation of a pharmaceutical or nutritional composition for use in the treatment and/or prevention of damage of the intestinal mucosa as a result of chemotherapy or radiotherapy, the pharmaceutical or nutritional composition comprising TGF-β and one or more binding factors for TGF-β in the substantial absence of insulin-like growth factor-1 (IGF-1) which TGF-β is obtainable by extraction from a mammalian milk whey product.
US7790771 Chloramine-t as a wound healing agent and viricide, particularly the herpes and varicella viruses; pruritus; skin disorders; diseasesof the mucous membranes, organs and tissues; with the exception of treatment of retro-viral (HIV) diseases; dermatitis; acne; psoriasis; side effect reduction The invention concerns the use of tosylchloramide(s), tosylchloramide salt(s), their derivatives and/or the decomposition products for treating diseases of the skin, mucous membranes, organs and tissues, excluding treatment of retroviral diseases (HIV) and disinfecting processes. It has been shown that tosylchloramide compounds can be used even for all diseases of the skin and viral mucosa causing formation of vesicles and itching, and they can lead to similar results as those obtained when they are used to treat corresponding diseases in tissues and organs. They not only provide quick relief of the acute symptoms and cure, but they also reduce frequency of recurrence. The inventive use is characterised in that it leads to very good treatment results, entirely independently of the form of preparation used, and it does not have to be administered in one specific manner. Relatively low amounts of tosylchloramide active principle can provide complete cure.
US20080279844 Methods for Treating Cancer Targeting Transglutaminase A method for treating cancer comprising inhibiting transglutaminase activity is provided. Suitable cancer types for which the methods of the present disclosure can be used to treat include, but are not limited to, pancreatic, breast, and ovarian cancers and melanoma. The inhibition of transglutaminase activity may be performed by one or more techniques, including, but not limited to, downregulating transglutaminase expression, inhibiting TG2 translation, or blocking TG2 enzymatic activity, such as with a small molecule inhibitor or intracellular antibody (intrabody).
CN103405444A Application of Chukrasone A in medicaments for treating bladder cancer The invention discloses an application of Chukrasone A in preparing medicaments for treating bladder cancer, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluation finds that the Chukrasone A also has a significant inhibitory effect on the growth of human bladder cancer cell strains T-24. Therefore, the Chukrasone A can be used for preparing anti-bladder cancer medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating bladder cancer provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to bladder cancer cells.
US20100076000 Sulfoximine-substituted pyrimidines as cdk- and/or vegf inhibitors, their production and use as pharmaceutical agents This invention relates to pyrimidine derivatives of general formula I in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.
US20100204300 Anti-viral methods and compositions The instant disclosure relates to methods and compositions for silencing poxvirus gene expression and replication using RNA interference. In certain embodiments, the disclosure relates to methods of treating a subject with a poxvirus infection.
WO2008094027A1 Use of suramin to prepare a drug for inhibiting retinal and corneal neovascularization The present invention relates to the use of suramin, or a pharmaceutically acceptable salt thereof, to prepare a drug for inhibiting retinal and corneal neovascularization in a patient. The present invention also relates to a method for treating retinal and corneal neovascularization in a patient requiring such treatment, characterized in that it comprises administering to the patient, by injection, an effective amount of suramin or a pharmaceutically acceptable salt thereof.
EP1901755B1 New pharmaceutical compositions containing hyaluronic acid or its derivatives and collagenase for the topical treatment of wounds, burns and ulcers The present invention concerns new compositions containing hyaluronic acid or the derivatives thereof in association with the proteolytic enzyme collagenase (and relative pharmaceutical formulations) for the preparation of a dressing for topical treatment of various kinds of wounds, burns of varying depth, pressure sores, vascular ulcers and diabetic foot ulcers as well as for the treatment of hypertrophic and keloid scars.
US7399860 Manufacture of polyglutamate-therapeutic agent conjugates The invention provides new processes for preparing polyglutamic acid-therapeutic agent conjugates for clinical development and pharmaceutical use, and polyglutamic acid-therapeutic agent conjugates prepared by these processes.
US20090263474 Methods for Treating Autoimmune Diseases in a Subject and In Vitro Diagnostic Assays The invention provides a method for treating an autoimmune disease in a subject by administering an interferon antagonist and a Flt3 ligand (Flt3L) antagonist. The invention also provides compositions containing one or more interferon antagonists, and one or more Flt3L antagonists, an in vitro assay for determining a subject's risk for developing an autoimmune disease, and kits for use, inter alia, with the assay.
WO2014113839A1 A method for improving the wellbeing of an animal using a composition including vitamin k There is disclosed herein a method of improving the wellbeing, as herein defined, of an animal comprising administering to an animal an effective amount of a composition containing: vitamin K1, vitamin K2 or a mixture of vitamin K1 and vitamin K2, together with a physiologically acceptable carrier, excipient and/or diluent.
CN101879139A Enteric-coated preparation for treating digestive diseases and preparation method thereof The invention provides an enteric-coated preparation for treating digestive diseases and a preparation method thereof. The enteric-coated preparation is a troxipide enteric-coated preparation, and active ingredients of the enteric-coated preparation are troxipide. The enteric-coated preparation comprises troxipide enteric-coated micropills, troxipide enteric-coated tablets, troxipide enteric-coated hard capsules, troxipide enteric-coated soft capsules, troxipide enteric-coated granules, troxipide enteric-coated solid dispersoids and the like. The troxipide cannot be absorbed in the stomach, so the troxipide is prepared into the enteric-coated preparation, so that the absorption programs and state of the ordinary oral administration preparation are changed, the aim of releasing and absorbing medicaments after the medicaments reach intestinal positions is fulfilled, the bioavailability of the preparation can be improved, and simultaneously, the medicaments also can be prevented from disintegrating in the stomach to stimulate lesion sites of gastric ulcer and acute and chronic gastritis and aggravate symptoms of nausea and vomit of patients. After the troxipide is prepared into the enteric-coated preparation, the compliance of the patients and the curative effect can be improved, and the side effect is reduced.
US20050113332 Compositions and methods for treating an arthritic condition The present invention features compositions and methods for the treatment of an arthritic condition. The compositions contain a reduced folate compound and a cobalamin compound.
CN101311167A 1-phenyl glyoxaline alkane -2,4-dione derivates and uses thereof The invention relates to a compound with a structure as shown in formula I, salt which is acceptable in pharmacy and a preparation method thereof; the compound can be used as a medicine, particularly has the application as the medicine for treating diseases which is relative to glucolipid; wherein, the definition of all radicals is detailed in the specification.
CA2593432A1 Fast-disintegrating dosage forms of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene A fast disintegrating dosage form of varenicline comprising an effective amount of varenicline or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient, wherein the dosage form disintegrates in a patient's oral cavity in less than three minutes. Also provided are a method for reducing nicotine addiction, aiding in the cessation of, or lessening of tobacco use in a subject by administering to the subject an effective amount of the fast disintegrating dosage form of varenicline or pharmaceutically acceptable salts thereof; a method of treating a disorder or condition by administering an effective amount of the fast disintegrating dosage form of varenicline; and, various methods of manufacturing or forming an immediate dosage form of varenicline.
CN103372212A Quinazoline molecular targeted medicinal composition The invention provides a quinazoline molecular targeted medicinal composition and a method for preparing the quinazoline molecular targeted medicinal composition. The quinazoline molecular targeted medicinal composition comprises a quinazoline medicine, phospholipid, cholesterol, a long-circulating material and additives. The quinazoline molecular targeted medicinal composition provided by the invention has high encapsulation efficiency. By using the quinazoline molecular targeted medicinal composition, the medicine can stay for a long time during blood circulation and has long half life, the inconvenient frequent administration of the medicine can be avoided, the function of the molecular targeted medicine (a tyrosine kinase inhibitor) can be strengthened, the apoptosis of tumor cells can be accelerated, and particularly the glioblastoma in the human brain can be inhibited better.
US20100086620 Bone Cement Composition and Method of Making the Same Disclosed herein is a composition suitable for use in spinal surgery. The composition generally includes a reaction product or settable mixture of first and second components, the first component including a spray-dried inorganic filler, a radical donor, and a pre-polymerized vinyl polymer, and the second component including a radical scavenger, a diluent, a polymerization accelerator, and a reactive monomer. Furthermore, disclosed herein is a method of making the composition, which generally includes mixing the first and second components under conditions suitable to form a curable reaction product.
CA2694401C Polycyclic compound Disclosed is a compound represented by the formula (I): (see formula I) or a pharmacologically acceptable salt thereof, which is effective as a therapeutic or prophylactic agent for a disease induced by A.beta., wherein Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group, or the like; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group, or the like; X1 represents a double bond, or the like; and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, or the like.
CN1993120A Arylacetic acids and related compounds for treatment of alzheimer's disease Compounds of formula I are useful in treatment of diseases associated with the deposition of ss-amyloid in the brain.
CN101513424B An injection for treating unknown high fever of pig An injection for treating unknown high fever of pig is characterized in comprising the following components: 50-150g of daimeton, 20-40g of trimethoprim, 400-800g of alpha-pyrrolidone, 30.5-50g of polyvinylpyrrolidone, and the balance of water. The advantages of the invention with simple process are in that: 1. the unknown high fever of pig can be effectively treated; 2. retention time of the sulfa drug is prolonged, thereby, the drug can be slowly released in vivo to achieve the long acting function.
CN102961381A Levofloxacin complex preparation and preparation method thereof The invention relates to a levofloxacin complex preparation. The levofloxacin complex preparation is characterized by comprising 10-20 parts of levofloxacin and auxiliary ingredients, and the auxiliary ingredients comprise 5-10 parts of ampicillin sodium, 3-5 parts of gentamicin sulphate or 3-5 parts of amoxicillin. According to the levofloxacin complex preparation, the levofloxacin and auxiliary ingredients are organically combined together, all components are coordinated and effected, the drug resistance of bacteria to the levofloxacin can be reduced, the antibacterial spectrum of the levofloxacin can be extended, the treatment effect can be improved, the clinical trials show that the levofloxacin complex preparation has stronger killing action on escherichia coli, salmonella, staphylococcus aureus, streptococcus pneumoniae, penicillin-resistant strain and the like, thereby being a preparation with high-efficiency and broad-spectrum antibacterial functions.
US7759392 4-nitroxybutyric acid ester derivatives of drugs such as acetaminophen, having an improved therapeutic index (efficacy/toxicity ratio) or a lower risk/benefit ratio, usedfor treating oxidative stress and endothelian dysfunctions, inflammation and pain Compounds or their salts of general formula (I): A-B—N(O)s wherein: s is an integer equal to 1 or 2; A=R-T1-, wherein R is the drug radical and T1=(CO)t or (X)t′, wherein X═O, S, NR1c, R1c is H or a linear or branched alkyl or a free valence, t and t′ are integers and equal to zero or 1, with the proviso that t=1 when t′=0; t=0 when t′=1; B=-TB-X2—O— wherein TB=(CO) when t=0, TB=X when t′=0, X being as above defined; X2 is equal to R1B—X—R2B radical wherein X is as above defined, R1B and R2B, equal to or different from each other, are linear or branched C1-C6 alkylenes, or X2 is a radical wherein two alkylene chains C1-C4 are linked to nonadjacent positions of a central ring having 4 or 6 atoms, said ring being an unsaturated cycloaliphatic ring, or a saturated or aromatic heterocylic ring, containing one or two heteroatoms, equal or different, selected from O, S, N; wherein the unsaturated cycloaliphatic ring does not have aromatic character according to Huckel's rule.
EP1720544A1 Novel azabicyclic derivatives, preparation method thereof and pharmaceutical compositions containing same The invention relates to compounds having general formula (I), the enantiomers and diastereoisomers thereof, as well as their addition salts with one or more acids or one or more pharmaceutically-acceptable bases. The inventive compounds are of particular interest for their interaction with central histaminergic systems.
CN1899400B Detection method for injection containing ginseng and aconite root in raw material The present invention relates to a kind of medicine preparation with ginseng component and aconite root component and its preparation process and quality control method. Of the medicine preparation, each unit contains total ginsenoside in 1-90 mg, total ginseng polysaccharide in 2-282 mg, and total aconite root alkaloid in 0.02-22 mg. The medicine preparation may have other synergistic medicine component added. Its preparation process includes extracting the total ginsenoside, the total ginseng polysaccharide and the total aconite root alkaloid; adding supplementary material; and forming different preparation forms.
CA2412845C Enhancement of antibody-cytokine fusion protein mediated immune responses by combined treatment with immunocytokine uptake enhancing agents Disclosed are compositions for treating tumors and the use of such compositions. Disclosed compositions enhance the uptake of immunocytokines into tumors, and are based on a combination of an immunocytokine with an immunocytokine uptake enhancing agent. The immune uptake enhancing agent is taxol, docetaxel, 10-deacetyl Baccatin III, cyclophosphamid or carboplatin, and can be administered to a mammal prior to the immunokine. Disclosed compositions are particularly useful for reducing tumor size and metastasis in a mammal.
WO2013124158A1 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors The present invention relates to the 1 H-indazole-3-carboxamide compounds having the following general formula (I) as glycogen synthase kinase 3 beta (GSK-3ß) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; (viii) epilepsies; and (ix) neuropathic pain.
CN101049334A Pale rose color drop pills A fast-release Yinhong dripping pill for treating cardiovascular and cerebrovascular diseases is prepared from safflower and gingko leaf through extracting carthamic yellow from safflower and ginkagetin from gingko leaf, and shaping.
WO2005123736A1 Novel 2-benzylaminodihydropteridinones, method for producing them and use thereof as drugs The invention relates to the novel 2-benzylaminodihydropteridinones of general formula (I), wherein the groups R1 to R7, R10 and R11 are defined as in the claims and in the description, and to the isomers thereof. The invention also relates to a method for producing said dihydropteridinones and to their use as drugs.
CN103356489A Proton pump inhibitor enteric coated pellet and preparation and preparation method thereof The invention relates to the field of medicines, especially to a proton pump inhibitor enteric coated pellet and a preparation and a preparation method thereof. The proton pump inhibitor enteric coated pellet is composed of a blank pellet core, a drug loaded layer, a protective layer, a separating layer, a waterproof layer and an enteric coating, wherein the waterproof layer is made from zein, the drug loaded layer is composed of a proton pump inhibitor, a first binder, a first stabilizing agent, a first antiadherent and a solubilizer or of the proton pump inhibitor, the first binder, the first stabilizing agent, a filler, a disintegrating agent and a first opacifier, the protective layer is composed of a second binder, a second stabilizing agent, a plasticizer, a second opacifier and an antifoaming agent, the separating layer is made of a coating material, and the enteric coating is composed of an enteric material, a plasticiser and a second antiadherent. The proton pump inhibitor enteric coated pellet and the preparation thereof in the invention have stable properties, reliable quality and high bioavailability and can avoid burst effects and moisture absorption.
EP2242737A1 Pregabalin salts Pharmaceutically acceptable acid addition salts of pregabalin that are isolatable in solid state, particularly crystalline state, sufficiently soluble in water, and stable both in the solid state and in the solution, as well as methods of making the salts and pharmaceutical compositions comprising the salts.
WO2011066379A2 METHOD OF REDUCING INTRATUMORAL pHe AND ACID-MEDIATED INVASION A method of treating cancer or inhibiting metastasis in a subject by reducing intratumoral extracellular pH. The method includes the step of administering to the subject a therapeutically effective amount of a buffer having a pKa greater than 6.1. In an advantageous embodiment the pKa of the buffer is about 7.0. Examples of buffers for reducing extracellular pH include NaHCO3, the buffer is selected from the group consisting of 2-imidazole-1-yl-3-ethoxycarbonylpropionic acid (IEPA), cholamine chloride, N,N-Bis(2-hydroxyethyl)-2-aminoethanesulfonic acid (BES), N-Tris(hydroxymethyl)methyl-2-aminoethanesulfonic acid (TES) and 4-(2-Hydroxyethyl)piperazine-1-ethanesulfonic acid (HEPES). The method can further include the step of pretreating with one or more chemotherapeutic agents.
CN101361831B New use of geniposide in preparating drug of vascular dementia treatment The invention belongs to the medicinal field, in particular to a new application of Gardenia. The technological problem needed to be solved is to provide the new medicinal application of the Gardenia, namely the application in preparing medicines for curing vascular dementia. Proved by experiments, after the inventor adopts a permanent bilateral common carotid artery ligation method and establishes animal models of the vascular dementia and cures the animal models for a month by giving different dosages of geniposide and positive control drug, the inventor carries out behavior and pathological observation for observing the influence of behavior and pathological brain tissue and related biochemical parameters of the geniposide on dementia rats. The inventor finds out that the geniposide with different dosages has functions of improving and recovering cognitive dysfunction of the vascular dementia rats and the rats have dose-dependency, wherein, the geniposide with medium and high dosages has the function of curing the dementia close to donepezil. Therefore, the Gardenia or the geniposide can be adopted for curing the vascular dementia.
CN101081817A Novel O-demethylated-venlafaxine maleate The present invention provides one new salt of O-demethyl-venlafaxine, O-demethyl-venlafaxine maleate, and its medicine composition.
US20080280974 Spiro compounds for treatment of inflammatory disorders Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof: wherein Y, Z and R1-R12 are defined herein.
CN103405781A Pharmaceutical composition of compound clindamycin and tazarotene lipid complex The invention provides a lipid complex of tazarotene and clindamycin phosphate. The lipid complex is prepared mainly by utilizing synthetic phospholipids and stearamide, is wrapped with tazarotene and is further mixed with the clindamycin to prepare cream and gel which are mainly used for treating acne vulgaris. The lipid complex is simple in preparation technique, and the stability of pharmaceuticals can be ensured in the preparation process; compared with the common cream and gel, the lipid complex has the advantages that the skin medicine retention volume is higher, the content of medicine in local skins can be increased, and the therapeutic index can be improved.
CN101497640B Novel crystal form of clofarabine The invention relates to a new crystal form of clofarabine, in particular to a clofarabine crystal form I with simple preparation process and better stability. The crystal form does not contain water and organic solvent, the X-ray powder diffraction spectra is shown in the attached drawing 1, and the melting point is 235.0 DEG C; and the invention also provides a preparation method for the clofarabine crystal form I, and the method comprises the following steps: the clofarabine with the amorphous I form is recrystallized in water, and then the obtained crystal is dried and dehydrated in vacuum. The provided clofarabine crystal form I containing no water and organic solvent has very good stability, is stable under strong light, is still stable after standing for ten days at a high temperature of 60 DEG C, can stand for half a year after being packaged by a polyethylene plastic bag at normal temperature and has stable physicochemical properties.
US20130023569 Use of Deferiprone for Treatment and Prevention of Iron-Related Eye Disorders There is provided use of orally available or topically applied deferiprone for prevention of iron-induced eye damage. The use may be for preparation of a medicament or in a method of preventing iron-induced eye damage to an eye of a subject at risk for iron-induced eye damage, the method comprising administering a prophylactically effective amount of deferiprone to the subject. There is also provided the use of deferiprone for treatment of iron-related eye disorders. The use may be for preparation of a medicament or in a method of treatment of damage to an eye of a having eye damage associated with iron, the method comprising topically administering a therapeutically effective amount of deferiprone to the subject.
DE102004050910A1 Composition containing phospholipid, sterol and negative charge carrier, useful e.g. for treating parasitic diseases and tumors, acts by stimulating leucopoiesis Pharmaceutical composition (A) comprises a phospholipid compound (A1); (7-beta -hydroxy)cholesterol and/or beta -sitosterol (A2) and a negative charge carrier (A3). Pharmaceutical composition (A) comprises: (1) a phospholipid compound (A1) of formulae (I)-(VII); (2) (7-beta -hydroxy)cholesterol and/or beta -sitosterol (A2); and (3) a negative charge carrier (A3), i.e. a 16-36C carboxylic acid, preferably saturated or mono-/poly-unsaturated, particularly with cis double bonds; a compound of the gallic acid type; an amide of a fatty acid (saturated, mono- or poly-unsaturated) or a fatty acid amide of glycerophosphoethanolamine, R1>O-P(=O)(O->)-(CH2)n-N+>R2>R3>R4> (I), a compound of formula (II), R1>O-CH2CH2-OP (III), R1>O-CH2-CH(OP)-(CH2)x-Me (IV), R21>O-CH2-CH(OR22>)-CH2OP (V), R31>O-CH2-C[(CH2)zH][(CH2)yH]-CH2OP (VI), R41>OCH2-C(Me)(OH)-CH2OP (VII), and R51>-CONHCH2CH2OP(=O)(O->)-OCH2CHOH-CH2OH (VIII) R1>, R11>, R21>, R31>, R41>15-26C (un)saturated hydrocarbyl; R2>, R3> and R4>H, 1-6C alkyl, 3-6C cycloalkyl or 2-6C hydroxyalkyl, or two of them together form 2-5C alkylene; n : 2-6; R12> and R13>H, 1-6C alkyl or 2-4C hydroxyalkyl; m : 1 or 2; x : 0-4; R22>1-6C alkyl; y and z : 0-3, but not both 0; R51>15-25C hydrocarbyl; P : PI or PII; Provided that in (IV) positions of R1> and P may be exchanged and in (V) R21>, R22> and P = may occupy any positions in the glycerol molecule. Independent claims are also included for the following: (1) use of erufosin (not identified) for treating tumors; (2) (VI) as new compounds; and (3) method for preparing (A1) that uses plant oil, especially olive oil, as starting material. [Image] - ACTIVITY : Parasiticide; Cytostatic; Protozoacide; Ophthalmological; Fungicide; Immunosuppressive. No details of tests for these activities are given. - MECHANISM OF ACTION : None given.
EP2206709A2 Thiophene derivatives as antiviral agents for flavivirus infection The present invention provides novel compounds represented by formula I or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
WO2008016118A1 Agent targeting dopamine receptor and screening method therefor It is intended to obtain a new finding related to a mechanism of inducing differentiation of Th1/Th2/Th17 through dendritic cells, and to provide a pharmaceutical effective in an immunity-related disease by utilizing the finding, a screening method for the pharmaceutical, and an effective agent for regulating a mechanism of inducing differentiation of Th1/Th2/Th17 through dendritic cells. The invention relates to a pharmaceutical for treating or preventing a disease caused by the imbalance of Th, characterized by containing a compound that modifies the activity of dopamine receptor as an active ingredient, a screening method for the pharmaceutical, and various agents characterized by containing a dopamine D1-like receptor antagonist or a dopamine D2-like receptor antagonist as an active ingredient.
CN101269044A Minocycline hydrochloride sustained-release dropping pill and preparation method thereof The invention discloses a pharmaceutical preparation used for high-efficiency and long-acting antibiosis, and particularly relates to a prepared sustained-release oral formulation adopting minocycline hydrochloride as the ingredient. The pharmaceutical preparation aims to supplement the deficiency of the prior art and provide a sustained-release minocycline hydrochloride dropping pill formulation. The sustained-release minocycline hydrochloride dropping pill can overcome the defects in the prior art effectively, guarantee no occurrence of an obvious quality change for the drug during the effective storage period and have the advantages of controllable release time, full release and high bioavailability simultaneously.
US20080045583 Stable levetiracetam compositions and methods Stable, liquid compositions of levetiracetam that are substantially or entirely free of preservatives, particularly parabens, and/or sugars, such as natural sugars and sugar alcohols. The liquid compositions preferably include oral solutions or suspensions, and may include pharmaceutically acceptable excipients.
CN102786575A Diosgenin-3-derivative as well preparation method and application thereof The invention relates to a diosgenin-3-derivative of general formula (1) as well the preparation method and application thereof. The R in the general formula (1) represents an amino acid group such as the glycine group, the L-alanine group, the 4-aminobutyrate group, the 2-aminoglutaric acid group (D-glutamic acid group) and the 6-aminocaproic acid. The derivatives which are the 4 6-aminocaproic acid diosgenin ester and the 7 2-amino-15-glutarate diosgenin ester are novel compounds. The detailed preparation method of the diosgenin-3-derivative is shown in the description. The diosgenin-3-derivative has the advantages that: a series of amino acid diosgenin esters or salts thereof are designed and prepared, the source of raw materials is abundant, and the preparation method of the diosgenin-3-derivative adopts simple steps for synthesizing, has high yield and is suitable for industrial production. The compound is stable in weak acid environment and is easy to be prepared into salt, and the solubility of the diosgenin is improved. The diosgenin-3-derivative is superior to the diosgenin in inflammation diminishing and tumor resisting activity. The diosgenin-3-derivative is mainly used for diminishing inflammation and resisting tumors.
US20070021419 2-Aminophenyl-4-phenylpyrimidines as kinase inhibitors The present invention relates to compounds of formula I, or pharmaceutically acceptable salt thereof, wherein: Z is CR10 or N; one of R1 and R2 is selected from (CH2)mR11, (CH2)mR12, (CH2)mNR12R13, (CH2)mOR12, (CH2)mNR13CO(CH2)nR11, (CH2)mNR13COR12, (CH2)mCONR13(CH2)nR11, (CH2)mCONR12R13, (CH2)mCO(CH2)nR11 and (CH2)mCOR12; where m is 0, 1, 2, 3 or 4 and n is 1, 2, 3 or 4; the other of R1 and R2 is H or R11; R3 and R5 are both H; R4 is H or R11; R6is H or (CH2)pR11, where p is 0 or 1; R7, R9 and R10 are each independently H or R11; R8 is selected from H, halogen, NO2, CN, OR13, NR13R14, NHCOR13, CF3, COR13, R13, CONR13R15, SO2NR13R14, SO2R13, NR13SO2R14, OCH2CH2OH, OCH2CH2OMe, morpholine, piperidine, and piperazine; each R11 is independently halogen, NO2, CN, (CH2)qOR13(CH2)rNR13R14, NHCOR13, CF3, COR13, R13, CONR13R14, SO2NR13R14, SO2R13, OR12, NR13SO2R14, OCH2CH2OH, OCH2CH2OMe, NR13SO2R12, (CH2)sNR12R13, morpholine, piperidine or piperazine, where q, r and s are each independently 0, 1, 2, 3 or 4; each R12 is independently a hydrocarbyl group optionally containing one or more heteroatoms and optionally substituted with one or more R11 groups; each R13 and each R14 is independently H or an alkyl group; and R15 is an alkyl group; providing that when Z is CR10 and R9 is H, at least one of R7, R8 and R10 is other than OMe; and Z is CR10 and R7-9 are all H, R10 is other than OCF2CHF2.
US20110098219 System for Curing Hepatic Cancer with Leptin The present invention cures hepatic cancer by MPA with the help of leptin. A therapeutic drug of MPA combined with leptin is applied to a liver cancer patient. Or, MPA can be directly applied to a patient having a high leptin expression. Or, if a patient has a low leptin expression, MPA is applied to the patient after leptin expression is increased. Hence, expression of leptin can be taken as a predictive factor and a prognostic factor of treatment effect on curing the patient with MPA.
CN102813842A Preparation method of freckle removing tincture The invention relates to a preparation method of freckle removing tincture. The preparation method includes: finely chopping motherwort, folium isatidis and Puccinellia tenuiflora, finely mashing with smoked plum, almond, walnut kernel, radix angelicae dahuricae and the like, soaking in alcohol, shaking until medicine juice seeps, and applying the tincture to facial parts with freckles. Long-term application of the freckle removing tincture can evidently remove freckles, chloasma, tinea versicolor and the like.
CN1568980A Dripping pills of compound allantoin The invention discloses a compound oral preparation by using ureidohydantoin and aluminum hydroxide as the pharmaceutical compositions, wherein the compound ureidohydantoin drop pill is prepared by using ureidohydantoin and aluminum trihydrate as active pharmaceutical raw material and mixing with matrix material according to a finite proportion.
US20110039859 Susceptibility to bone damage In one aspect, the present invention provides methods for determining susceptibility to bone damage in a subject. In some embodiments, the methods comprise screening for polymorphisms in the MTHFR and collagen Iα1 genes that are associated with susceptibility to bone damage. In some embodiments, the methods comprise screening for elevated levels of homocysteine in a subject, wherein elevated levels of homocysteine are associated with an increased risk of bone damage. The methods of the invention may be used in predicting the response of a patient to treatment. Also provided are methods for prevention or reducing the risk of bone damage in a subject.
EP1856105A1 Quinoxaline dihydrohalide dihydrates and synthetic methods therefor Crystalline polymorph forms of Gonadotropin Releasing Hormone receptor antagonists, including crystalline polymorphs of quinoxaline dihydrohalide dihydrates, in particular crystalline polymorphs of 6-({4-[2-(4-tert-butylphenyl)-lH-benzimidazol-4-yl]-piperazin-l- yl}methyl)-quinoxaline dihydrochloride dihydrate, methods of making the same, as well as pharmaceutical compositions, and dosage forms containing them are disclosed.
US20120164207 Degradable networks for sustained release and controlled release depot drug delivery applications Provided herein is a controlled release and/or sustained release depot drug delivery system, comprising, a biodegradable polymer coating and an API coated with the biodegradable polymer coating, wherein a quantity of API coated with biodegradable polymer is effective to be released from the biodegradable polymer coating over a prolonged period of time.
CN103040863A Disodium clodronate liposome injection The invention discloses disodium clodronate liposome injection and a preparation method thereof. The disodium clodronate liposome injection with excellent quality is made of disodium clodronate, distearoyl phosphatidyl glycerol, cholesterol, polyoxyethylene (40) hydrogenated castor oil according to specific weight ratio. Compared with the existing preparation, the injection has the advantages that the stability and the bioavailability of the injection are greatly improved, drug release is stable, the quality of injection products is improved, the toxic and side effect is reduced, and the curative effect is more obvious.
WO2011033470A1 Crystalline form of montelukast sodium The present invention relates to a crystalline form of montelukast sodium. The crystalline form of montelukast sodium is designated as Form D1. The present invention also relates to a process for preparing crystalline montelukast sodium. The present invention further relates to a pharmaceutical composition comprising crystalline Form D1 of montelukast sodium and its method of use.
WO2007014137A3 8-carboxamido-substituted-2 , 6-methano-3-benzazocines and 3 - carboxamido- substituted morphanes as opioid receptor binding agents 8-Substituted-2,6-methano-3-benzazocines of general structure; formula (I) are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti- addiction medications. One embodiment is the subgenus of biphenylethyl compounds; formula (II).
CN103751142A Butoconazole nitrate vaginal effervescence tablet The invention provides a butoconazole nitrate vaginal effervescent tablet including butoconazole nitrate, a filler, a foaming agent and a foam stabilizer, and the butoconazole nitrate accounts for 20-60 wt% in the vaginal effervescent tablet. The foaming agent comprises an acid system comprising acid or acid salt, and an alkali system comprising carbonates. The acid system includes citric acid, tartaric acid, succinic acid, fumaric acid, adipic acid, malic acid, water-soluble amino acid, potassium bitartrate, sodium hydrogen tartrate, sodium bitartrate, potassium dihydrogen citrate, sodium fumarate and boric acid. The alkali system includes sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate, calcium bicarbonate and calcium carbonate. The foam stabilizer is a surfactant selected from sodium dodecyl sulfate and Tween 80. The butoconazole nitrate vaginal effervescent tablet provided by the invention can be used for treating vaginal infection diseases caused by candida.
CN1876011A A pharmaceutical composition capable of improving boar reproductive performance The invention discloses a medicinal composition for increasing pig's reproductive performance, which is prepared from glycerin, olive oil, spinacene and dried wheat flour.
CN103550220A Long-acting injection containing enrofloxacin hydrochloride and ceftiofur hydrochloride The invention relates to preparation for applying sucrose acetate isobutyrate to veterinary oil injections and particularly relates to preparation for applying a combination of sucrose acetate isobutyrate and hydrogenated castor oil or a combination of sucrose acetate isobutyrate and aluminum stearate to a compound long-acting injection containing enrofloxacin hydrochloride and ceftiofur hydrochloride, wherein a dispersion medium of the injection is isopropyl myristate, ethyl oleate or a mixture of benzyl benzoate and ethyl oleate. The injection has the advantages of good slow-release effect, stable property, good histocompatibility and easiness in preparation.
US20080032954 Vascular Damaging Agents for Administration as an Intravenous Infusion The invention concerns the use of a vascular damaging agent or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for administration as an intravenous infusion to a warm-blooded animal such as a human over a time period of more than 1 hour for use in the production of a vascular damaging effect in said warm-blooded animal. The invention also concerns kits adapted for intravenous infusion of a vascular damaging agent over a time period of more than 1 hour and to methods for providing a vascular damaging effect in a warm-blooded comprising administering a vascular damaging agent to the warm-blooded animal over a time period of more than 1 hour.
CN101040841A Anticancer compound including phosphatidylinostitol 3-kinase inhibitor and alkaloid The invention relates to an anti-cancer compound as a slow release injection which contains phosphoinositide 3-kinase restrainer and/or alkaloid, formed by slow release micro ball and solvent. The slow release micro ball comprises the anti-cancer effective components and slow release findings, selected from phosphoinositide 3-kinase restrainer and/or alkaloid, the solvent is a common solvent or a special solvent with suspending agent, while the viscosity of suspending agent is 100cp-3000cp (at 20-30Deg. C), selected from carboxymethyl cellulose, the anti-cancer effective component is phosphoinositide 3-kinase restrainer and/or the phosphoinositide 3-kinase restrainer booster selected from self-anti-cancer antibiotics and/or tetrazine drug, the slow release finding is selected from phosphate polyester as p (LAEG-EOP), p (DAPG-EOP), p (BHET-EOP/TC), p (BHET-EOP/TC), p (BHDPT-EOP/TC), p (BHDPT-EOP/TC), p (CHDM-HOP) or p (CHDM-EOP), or the polyester or mixture of phosphate and polylactic acid, polyphenyl, 2-aliphatic acid, sebacic acid polyester, poly (erucic acid dimmer-sebacic acid) or poly (fumaric acid-sebacic acid). The anti-cancer compound can be made as slow release plant agent, to inject cancer or around cancer to hold the effective drug density for more than 40 days, while it can significantly reduce the general reaction of drug and selectively strengthen the effect of non-surgery treatments as chemotherapy or the like.
US20130017274 Low dose lithium in the treatment or prophylaxis of parkinson's disease In various embodiments methods of delaying the onset of and/or mitigating the severity of one or more symptoms of Parkinson's disease in a mammal are provided. In certain embodiments the methods involve administering to a mammal diagnosed as having or as at risk for Parkinson's disease a chronic low dose of lithium (e.g., a subtherapeutic dose). In certain embodiments the low dose lithium is administered in conjunction with another agent (e.g., L-DOPA).
WO2008034516A1 Antibiotic maduraphthalazin salts with delayed release of the active substance and their use The invention describes antibiotic maduraphthalazin salts that show a low solubility in water and a delayed release of the active substance and are characterized by the fact that they consist of an anionic component, which is formed by at least one representative of the group of carboxyalkylated or carboxyarylated maduraphthalazins and of a cationic antibiotic component. In human and veterinary medicine, the antibiotic maduraphthalazin salts that show a low solubility in water can be used in permanent or temporary implants and as an element of implant coatings in the fight against bacterial infections at a specific location and in the prophylaxis against infections.
WO2006043846A1 Salt of montelukast with tert.-butylamine The invention relates to a novel salt of montelukast with tert-butylamine and its use in the process for the preparation of highly pure free montelukast acid and/or pharmaceutically acceptable salts thereof, in particular montelukast sodium.
WO2011096808A1 Use of sialyl oligosaccharides in weight management The invention relates to prebiotics and the use thereof for promoting human health. In particular, it relates to milk-, whey- or egg-derived oligosaccharides capable of enhancing the relative abundance of beneficial micro-organisms. Provided is the use of a sialyl - oligosaccharide for the manufacture of a dietetic, nutraceutical, pharmaceutical or nutritional composition, like an infant formula, for treating or preventing a condition associated with a reduced amount of Bacteroides ssp. in the gastrointestinal tract. Also provided is an infant formula for reducing the risk of development of overweight or obesity of an infant in later life. Said composition comprises living Bacteroides ssp. in an amount of at least 10+5cfu/g dry weight of the composition.
WO2010037536A1 N-protected guanidine-substituted furans, thiophenes, and pyrrols as cysteine protease inhibitors The present invention relates to N-protected guanidine-substituted furans, thiophenes, and pyrrols, to the use thereof as cysteine protease inhibitors, to pharmaceutical compositions containing said compounds, and to the use thereof for the treatment of autoimmune diseases, parasitic diseases, and cancer.
US20090163566 Imidazole Derivatives and their use for Modulating the Gabaa Receptor Complex This invention relates to novel imidazole derivatives of the general formula (I): pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
US6919317 For therapy of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g.skin plays a role Synergistic combinations of a squalene epoxidase inhibitor such as terbinafine and a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro, 33-desoxyascomycin are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin plays a role, such as atopic dermatitis and seborrhoeic dermatitis, and in situations of fungal resistance.
CN102603751A Triazol (4,5-D) pyrimidine derivate and preparation method of triazol (4,5-D) pyrimidine derivate as well as application of triazol (4,5-D) pyrimidine derivate in drug preparation The invention discloses a triazol (4,5-D) pyrimidine derivate and a preparation method of the triazol (4,5-D) pyrimidine derivate as well as application of the triazol (4,5-D) pyrimidine derivate in drug preparation. The derivate is a compound as shown in a formula I. A pharmacodynamic test result shows that the compound shown in the formula I has the remarkable effect of inhibiting platelet aggregation. Therefore, the compound of the formula I can be used for preparing drugs for preventing or treating thrombus and embolism related diseases. The invention also provides the preparation method of the compound of the formula I.
US20050101530 Cellular virus receptors and methods of use Methods, reagents and compositions for the treatment, prevention and diagnotic of virus infections in vertebrates and more paticularly in human and animals are described. The invention provides evidence that the CCR1, CCR2, CCR3, CCR4, CCR5 and CCR8 receptors are involved in human respiratory syncytial virus (RSV) infections. Therefore, the present invention describes methods for modulation of cellular viral infection by modulating a binding interaction between a CCR1, CCR2, CCR3, CCR4, CCR5 and/or CCR8 receptor and a surface protein of the virus. The invention also profits of such a binding interaction for 10 providing methods for reducing viral infection of a cell; methods of attenuating the ability of a pneumovirus to bind a mammalian cell; methods for reducing the initiation or spread of a respiratory tract disease due to human RSV; methods for detecting the presence of a pneumovirus in a biological sample; gene therapy methods, and methods for identifying novel antiviral and anti-inflammatory 15 compounds.
US20050244381 Adenovirus including a gene coding for a superoxide dismutase A defective recombinant adenovirus including at least one DNA sequence coding for all or an active part of a superoxide dismutase or a derivative thereof. The therapeutical use thereof and corresponding pharmaceutical compositions are also disclosed.
CN1813719A Astemizole dropping pill and its preparing method The present invention discloses a medicine astemizole dripping pills preparation for effectively curing the diseases of perennial and seasonal anaphylactic rhinitises, allergic conjunctivitis, chronic urticaria and other anaphylactic reactive symptom and sign and its preparation process. Said astemizole dripping pills preparation is made up by using astemizole and dripping pill matrix.
CN103429590A 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors The present invention relates to 1,4 Thiazepines/Sulfones of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
EP1010701B1 Process for the preparation of 3-cephem compounds A process for the preparation of 3-cephem compounds, characterized by reacting a β-lactam compound represented by general formula (1) with a phosphorus halide compound in the presence of an organic base to form an imino-β-lactam compound represented by general formula (2), adding a phenol to the resulting reaction system to conduct alcoholysis simultaneously with the deblocking of the carboxylate ester, and thus obtaining a 3-cephem compound represented by general formula (3) or a salt thereof, wherein R1, R2, R3 and X are each as defined in the description.
WO2013126608A1 Sulfonamide compounds and uses as tnap inhibitors Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper- mineralization.
EP2432770A1 Benzenesulfonanilide compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor The present invention relates to novel benzenesulfonanilide compounds of the Formulae (I) and (I') and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. (I) (I') F wherein R1 is hydrogen or methyl; R2 is hydrogen or methyl and is positioned vicinal to the radical R1; R3 hydrogen, C1-C3 alkyl, halogen, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R4 is hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, C3-C4 cycloalkylmethyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, chlorine, C1-C4 alkyl, fluorinated C1-C4 alkyl, C1-C4 alkoxy or fluorinated C1-C4 alkoxy; and R6 is hydrogen, fluorine or chlorine.
CN102443009A Fused ring kinase inhibitor The invention belongs to the technical field of medicine, specifically relates to a fused ring kinase inhibitor represented by a general formula (I), pharmaceutically-acceptable salts of the fused ring kinase inhibitor, or stereoisomers of the fused ring kinase inhibitor, wherein R<1>, R<2>, R<3>, X, Y, Z, M, L or Q are described in the instruction. The present invention further relates to a preparation method for the compounds, and a use of the compounds in preparation of drugs for treatment and/or prevention of cancers.
WO2011014084A1 Use of 5h-dibenz / b, f/ azepine-5-carboxamide derivatives for treating fibromyalgia The use of 5H-dibenz/b,f/azepine-5-carboxamide derivatives for treating fibromyalgia. Useful 5H-dibenz/b,f/azepine-5-carboxamide derivatives include compounds of the formula (I): where R1 is hydrogen, alkyl, halogenalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkoxy, aryl, or pyridyl; the term alkyl means a straight or branched hydrocarbon chain containing from 1 to 18 carbon atoms; the term halogen means fluorine, chlorine, bromine or iodine; the term cycloalkyl means an alicyclic saturated group with 3 to 6 carbon atoms; and the term aryl means an unsubstituted phenyl group or phenyl substituted by alkoxy, halogen or nitro group.
CN102512426A Application of ursolic acid in preparation of health care product with effects of weight loss and fatty liver improvement The invention provides application of ursolic acid in preparation of a health care product with effects of weight loss and fatty liver improvement. The ursolic acid is found to be capable of remarkably reducing the weight of a big fat mouse induced by high fat diet and effectively improving fatty liver caused by obesity.
CN102451470A Oxymatrine phosphatide compound and preparation method and application thereof The invention discloses an oxymatrine phosphatide compound which is a compound comprising oxymatrine and phosphatide. The invention also discloses a method for preparing an oxymatrine phosphatide compound, which comprises the following steps: allowing oxymatrine and phosphatide to react in a reaction solvent. The invention also discloses an application of the oxymatrine phosphatide compound in the preparation of medicaments for inhibiting hepatitis B virus. The bioavailability of the oxymatrine phosphatide compound of the invention reaches above 328.57%. The preparation method of the present invention has a simple process, is applicable to industrial production, and has a compound rate of up to 80.2%.
CN101703604B Medicament for treating dermatophytosis The invention provides a medicament for treating dermatophytosis, and belongs to the technical field of medicaments. The medicament comprises the following components in part by weight: 100 to 300 parts of ethanol, 1 to 10 parts of shrubalthea bark, 1 to 5 parts of cicada slough, 5 to 20 parts of lightyellow sophora root, 5 to 15 parts of salicylic acid, 10 to 20 parts of swordlike atractylodes rhizome, 10 to 30 parts of amur cork-tree bark, 2 to 10 parts of peppermint, and 100 to 300 parts of Vaseline. The medicament can quickly relieve itching, reduce inflammation, repair skin, and promote wound healing of ulcered skin and cutin.
WO2011083264A1 Thiochroman derivatives, method for preparing same and pharmaceutical compositions containing same The invention relates to compounds of formula (I), where R1, R2, R3 and R4, identical or different, each represent a hydrogen atom, a halogen atom or a cyano, hydroxyl, thio, nitro, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, carboxyl, alkoxycarbonyl, aryloxycarbonyl, acyloxy, arylcarbonyloxy, acyl, arylcarbonyl, amino, arylamino, acylamino, arylcarbonylamino, aminocarbonyl, arylaminocarbonyl, alkylsulfonylamino, or arylsulfonylamino group. The invention can be used in the field of drugs.
US20090170933 Method for removing a medical device from a spasmodic constriction in a bodily passageway A method and apparatus for removing a medical device entrapped in a bodily passageway resulting from a spasmodic constriction of bodily tissue surrounding the device involves delivering to the site of the constriction an amount of an antispasmodic agent sufficient to relax the surrounding bodily tissue. The method may also be used for relaxing the tissue of a vessel wall to inhibit constriction of the vessel wall upon the introduction of a medical device into the vessel.
CN101870718A Preparation method of high-purity natural ursodesoxycholic acid and application thereof in medicament The invention belongs to the technical field of medical biology, in particular to a preparation method of high-purity natural ursodesoxycholic acid. The high-purity natural ursodesoxycholic acid is obtained by separating and purifying bear gall powder prepared from a manual drained bear gall, and the high performance liquid chromatography purity is not lower than 98 percent. The preparation method comprises the following steps of: firstly, separating and purifying by applying a cation exchange medium to prepare tauroursodeoxycholic acid with purity not lower than 90 percent; and then thoroughly hydrolyzing the tauroursodeoxycholic acid into ursodesoxycholic acid and taurine in the presence of alkali and separating and purifying by applying a silica gel adsorption chromatography technology to prepare the ursodesoxycholic acid with purity not lower than 98 percent. The natural ursodesoxycholic acid prepared by the invention has the effects on treating primary biliary cirrhosis and primary sclerosing cholangitis.
EP1904058A2 Combination of a dpp-iv inhibitor and a cannabinoid cb1 receptor antagonist The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and comprising at least one CB1 antagonist, or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention of, delay of progression of, treatment of diseases and disorders that may be inhibited by DPP IV inhibition, appetency disorders or substance abuse disorders.
CN1986525A 4-methoxy-1,3-phenyl disulfamide derivative and its application The present invention synthesizes 4-methoxy-1, 3-phenyl disulfamide derivative and its structural analog based on new medicine designing theory and principle. The target compound has its structure confirmed by means of its infrared spectrum and nuclear magnetic resonance spectrum. The compound of the present invention, platelet aggregation antagonizing test shows, has obvious platelet aggregation promoting activity. The compound of the present invention may be used in medicine composition for promoting or antagonizing platelet aggregation.
US20080125426 7-(4-Chlorophenyl)-4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile; reversible inhibitors of cysteine proteases S, K, F, L, B; diseases associated with Cathepsin S; antiinflammatory agent, autoimmune diseases; asthma, rheumatoid arthritis, multiple sclerosis, Alzheimer's and Crohn's disease The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.
EP2526103A1 A process for the preparation of novel porphyrin derivatives and their use as pdt agents and fluorescence probes The present invention provides novel porphyrin derivatives represented by the general formula 1 and /or pharmaceutically acceptable derivatives thereof as NIR sensitizers for photodynamic therapeutic and diagnostic, biological and industrial applications. These porphyrin derivatives posses absorption (400-700 nm) and emission (600-750 nm) in the regions where biological chromophores do not absorb and hence are ideal candidates for application as NIR PDT agents and fluorescence sensors for medicinal applications in biology. The substituents like hydroxyl and glycolic units on these dyes render them amphiphilicity thereby improving their solubility in the aqueous media and cellular uptake and localization. These dyes show no toxicity in the dark and are highly selective towards tumor cells and stain nucleus very rapidly. Accordingly, these porphyrin derivatives are extremely useful as NIR PDT fluorescence sensors in photodynamic therapeutic and diagnostic, biological and industrial applications.
CN103520128A Pramipexole sustained-release tablet, preparation method and application thereof The invention discloses a pramipexole sustained-release tablet, a preparation method and application thereof. The sustained-release tablet is composed of pramipexole or pharmaceutical salts thereof, two or more water-swellable neutral polymers and other excipients, wherein the water-swellable neutral polymers comprise cellulose neutral polymers and non-cellulose neutral polymers; and the compositions of the sustained-release tablet comprise in percent by weight: 0.05-4% of pramipexole or pharmaceutical salts thereof, 5-90% of a cellulose neutral polymer, 4-93% of a non-cellulose neutral polymer and the balance other excipients. The sustained-release tablet comprises the following advantages that: the in-vitro dissolution release reaches the effect consistent with an original drug, and thus the sustained-release tablet is capable of possessing the clinical effect consistent with an original preparation; and anionic polymers used in the patent of the original preparation is abandoned, and thus the release and the absorption of the medicine in vivo are not influenced by pH value of gastric juice, and the disadvantages of the original preparation are avoided.
US20120088792 Pyridin-2-YL Methylamine Derivatives for Treating Opiate Dependence The invention concerns the use of compounds of general formula (I) for treating opioid drug dependence, hyperalgesia induced by opiate drug withdrawal and psychological craving induced by opiate drug withdrawal.
EP1054004B1 Novel pyrimidine-5-carboxamide derivatives Pyrimidine-5-carboxyamide derivatives represented by general formula (I) or salts thereof, wherein each symbol has the meaning as specified below: X: O, S, NR1, CO, NR1CO, CONR1, C=N-OR1 or a bond; Y: lower alkylene optionally substituted by OR1 or -NHR1 or a bond; Z: O, NR2 or a bond; A: H, optionally substituted lower alkyl, lower alkyl optionally having -CO-, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl or an optionally substituted and saturated heterocycle containing nitrogen; B: optionally substituted aryl or optionally substituted heteroaryl; and R1, R2: H or lower alkyl optionally having -CO-.
WO2013004556A1 A molecule regulating activity of insulin degrading enzyme (ide) The present invention relates to the treatment of Alzheimer's disease and type 2 diabetes mellitus by a small molecule changing the activity of IDE. The molecule binding to the exosite of insulin degrading enzyme accelerates amyloid-β cleavage.
EP2416655A1 Methods for preventing and/or treating degenerative disorders of the central nervous system The present invention provides methods for preventing and/or treating degenerative disorders of the central nervous system using 5- (fluoromethyl)piperdine-3,4-diol, 5-(chloromethyl)piperdine-3,4-diol, or a pharmaceutically acceptable salt, solvate, or prodrug thereof, or any combination of two or more thereof. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease.
EP2739279A2 Novel aniline derivatives and use thereof The present invention relates a novel aniline derivatives for anticancer and more particularly, it relates a novel aniline derivatives for anticancer comprising compound of the Formula 1 or a derivative thereof as an active ingredient. A compound of the present invention inhibits AIMP2-DX2 which is novel anticancer target and induces apoptosis of cancer cells, thereby being effective in preventing and treating cancer. Therefore, a novel aniline derivatives of the present invention can be used for preventing and treating cancer.
US20080153112 identification of a predominant ligand of CD8+ T cells that are responsible eq for type 1 diabetes. That ligand is islet-specific glucose-6-phosphatase catalytic subunit-related protein (IGRP). Several CD8+ T cell-binding peptides from IGRP are identified, including the peptide comprising amino acids The present invention is based on the identification of a predominant ligand of CD8+ T cells that are responsible eq for type 1 diabetes. That ligand is islet-specific glucose-6-phosphatase catalytic subunit-related protein (IGRP). Several CD8+ T cell-binding peptides from IGRP are identified, including the peptide comprising amino acids 206-214 of the IGRP sequence, which has high avidity to the most prevalent T cell receptor of pathogenic CD8+ T cells in autoimmune diabetes. The invention thus provides oligopeptide and polypeptide compositions comprising YLKTN/A/I/L/V)FL, FLWSVFWLI, (T/A)YY/G/T)FLNFM, LR(LV)(F/L)(G/N)IDLL, KWCANPDWI, and SFCKSASIP. Also provided are oligopeptide compositions 8-10 amino acids in length and completely homologous with a mammalian IGRP, where the oligopeptide is capable of binding a human MHC class I molecule. Additionally, various methods of treating a mammal using the above compositions are provided, where the mammal is at risk for or has type 1 diabetes. Also provided are methods of preventing a CD8+ T cell that is cytotoxic to pancreatic islet β-cells from destroying a mammalian β-cell, where the methods also use the above compositions. Further provided are methods for determining whether a mammal is at risk for or has type 1 diabetes, where the methods use the above compositions.
US7012080 Imidazopyridine compounds as 5-HT4 receptor agonists This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a methyl group or an ethyl group; R3 represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms; with the proviso that when the terminal carbon atom of said alkyl group of R3 is substituted by said alkoxy group, said alkyl group is a branched alkyl group. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
WO2013175479A1 Compositions comprising isosilybin b for amelioration and prevention of drug- induced toxicity Compositions comprising isosilybin B and optionally additional protective agents selected from methylsulfonylmethane (MSM), phosphatidylcholine (PC), cysteine (Cys), seleno-cysteine (Se-Cys), ribose-cysteine (RibCys), N-acetylcysteine (NAC), N- acetylcysteine-amide (AD4), methionine (Met) and S-adenosylmethionine (SAM) for use in reducing and / or preventing drug- induced toxicity, such as acetaminophen-induced toxicity. Said compositions further comprising acetaminophen for use as safe formulations of acetaminophen with reduced risk of causing liver damage.
CN102652744A Modified injection containing 13 compound vitamins and preparation method thereof The invention discloses a modified injection containing 13 compound vitamins and a preparation method thereof, and relates to the field of medicinal preparations. In order to solve the problems of poor stability and rigorous preservation conditions of similar injections in the prior art, the invention discloses a compound vitamin injection which is separatedly loaded in two ampoules, and comprises 4 fat-soluble vitamins and 9 water-soluble vitamins in total; meanwhile solubilizers, antioxidants and preparation technology of the compound vitamin injection are also modified. The compound vitamin injection prepared by the invention has significantly improved stability, and can be preserved for 18 months at room temperature.
WO2009105440A1 Beta-lactams for reducing intraocular pressure A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
US6984650 Comprises phosphorescence and fluorescence resonance energy transfer; binding chenodeoxycholic acid to farnesoid X receptors; for regulating cholesterol absorption; for treatment of obesity The present invention includes nuclear receptor heterodimer and nuclear receptor-coactivator peptide assays for identifying ligands for nuclear receptors, utilizing scintillation proximity and fluorescence resonance energy transfer (FRET), and methods of using identified ligands.
CA2313629C Method for transferring one or more active ingredients between different phase carriers The present invention relates to a method for transferring one or more active ingredients between different phase carriers, which includes: (a) providing a solid, semi-solid, or non-aqueous liquid drug which contains at least one active ingredient; (b) admixing said drug with water or water solution to form an admixture; and (c) nebulizing said admixture to form liquid fine drops containing said active ingredient. This method enables the active ingredient stored in a solid phase carrier to transfer into an aqueous phase carrier, or enables the active ingredient stored in a non-aqueous liquid carrier to transfer into an aqueous phase carrier. The aqueous phase carrier contains the active ingredient can then be nebulized with a nebulizer by means of ultrasonic vibration.The present invention provides a new method for controlling administration by transferring the active ingredient between different phase carriers.
US20100197732 Repaglinide Substantially Free of Dimer Impurity The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2-piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.
CN1562069A Use of C-ski gene and its polypeptide in preparing medicine for improving tissue repairing and reducing scar formation An application of c-ski gene and its polypeptide in preparing the medicines in the form of injection, liquid, emulsion, cream or ointment for treating the injury of epithelial tissue or other tissue and preventing the generation of residual scar is disclosed.
US8163305 Targeted cross-linked nanoparticles and their use in vivo gene delivery The in vivo delivery of nucleic acids is targeted by delivery of the nucleic acid in a complex with cross-linked nanoparticles; where the nanoparticles comprise cross-linked neutral amphipathic molecules, cationic amphipathic molecules and targeting amphipathic molecules. Optionally the cationic and targeting amphipathic molecules are also cross-linked. A targeting moiety present on the targeting amphipathic molecule provides for selective delivery of the complex to a predetermined target site, e.g. blood vessels, endothelial cells, tumor cells, liver cells, and the like.
CN102824355A Use of panax japonicus saponin IV a in preparation of alpha-glycosidase inhibitor The invention discloses a use of a panax japonicus saponin IV a in preparation of an alpha-glycosidase inhibitor. The panax japonicus saponin IV a is extracted from pure Aralia chinesis L. and has high activity of inhibiting alpha-glycosidase and alpha-amylase. An experiment proves that the panax japonicus saponin IV a can be used for preparation of an alpha-glycosidase inhibitor and an alpha-amylase inhibitor.
CN101422497A Ginsenoside Rb1 containing impurity Panax Notoginseng saponin R2 The invention discloses a standard active ingredient of a ginsenoside Rb1, which comprises the ginsenoside Rb1 with the content of more than or equal to 90 percent and less than 100 percent, and is characterized in that the content of the foreign substance of notoginsenoside R2 is more than 0 and less than 1 percent; or the content of the foreign substance of the otoginsenoside R2 is more than or equal to 0.01 percent and less than or equal to 0.5 percent. The pharmacological test indicates that the standard active ingredient of the ginsenoside has good pharmacological action and can be prepared into pharmaceutical preparation on pharmaceutics.
US20120252776 C4 Monomethyl Triterpenoid Derivatives and Methods of Use Thereof Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.
CA2850003A1 Broad-spectrum antivirals against 3c or 3c-like proteases of picornavirus-like supercluster: picornaviruses, caliciviruses and coronaviruses Antiviral protease inhibitors, including peptidyl aldehydes, peptidyl a-ketoamides, peptidyl bisulfite salts, and peptidyl heterocycles, are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus.
US20060182688 Metronidazole-based tinted topical pharmaceutical compositions Topically applicable pharmaceutical compositions suited for the treatment of dermatological complaints, conditions or afflictions, notably rosacea, contain a thus effective amount of metronidazole and at least one dye effective to impart a green color thereto, formulated into a topically applicable, pharmaceutically acceptable vehicle therefor.
WO2014134419A1 Use of ikach blockers for the treatment of cardiac diseases The present disclosure relates to methods of treating and/or preventing cardiac diseases in human patients by administration of an effective amount of one or more acetylcholine-activated potassium current (IKACh) blockers.
WO2011035540A1 4-(substituted anilino)quinazoline derivatives as tyrosine kinase inhibitors 4-(substituted anilino)quinazoline derivatives used as inhibitors of tyrosine kinase are disclosed. Specifically, compounds of formula I, pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent of formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are efficacious inhibitors of tyrosine kinase.
US20080003260 Use of 5-fluorourcil, delivered by iontophoresis as an inhibitor of cell proliferation in the eye, bulbar and palpebral conjunctiva, eyelid, peri-orbital soft tissues and skin A method for treating neoplastic, angiogenic, fibroblastic, and/or immunosuppressive ocular irregularities of a living subject, comprising the steps of: providing a living subject, wherein the living subject includes an affected ocular area having a neoplastic, angiogenic, fibroblastic, and/or immunosuppressive irregularity; providing a 5′ fluorouracil based medicament, wherein the 5′ fluorouracil based medicament is capable of inhibiting DNA synthesis; associating a therapeutically effective concentration of the 5′ fluorouracil based medicament with the affected ocular area of the living subject; and decreasing the neoplastic, angiogenic, fibroblastic, and/or immunosuppressive ocular irregularity of the living subject.
US20090011013 Tacrolimus Combination Products The present invention relates to a pharmaceutical composition comprising tacrolimus or an analogue thereof and a substance being a substrate for CYP3A4 and/or P-glycoprotein, oral solid dosage forms comprising the pharmaceutical composition such as tablets, methods for preparing the pharmaceutical composition and oral dosage forms and use of the pharmaceutical composition for preparing a medicament. The substance being a substrate for CYP3A4 and/or P-glycoprotein is preferably cyclosporine A. The invention further relates to treatment of a patient in need thereof by coadministration of the combination according to the invention. In a further aspect, the invention relates to the above combination further comprising a CYP3A4 inhibitor compound, preferably a compound naturally occurring in citrus juice, for example grapefruit juice, preferably a spiro ortho ester compound.
US20120121707 Tolbutamide Particle And Preparing Method Thereof And Method Of Reducing A Blood Glucose A method for preparing a tolbutamide particle is provided. The method comprises steps of mixing a bulk drug of tolbutamide with a supercritical fluid to form a supercritical mixture; and expanding the supercritical mixture to obtain the tolbutamide particle.
CN1961870A Method for preparing sustained releasing microcapsule of phenoxybenzamine hydrochloride and ethyl cellulose The invention relates to a method for preparing alcaine dibenzylin-ethyl cellulose slow-release capsule, wherein it breaks the alcaine dibenzylin into 40-100 deals, and breaks the ethyl cellulose whose viscosity is 10CP into 80-140 deals, while their mass percentages is 2:1-6:1; mixing and adding them into volatile solvent to be dissolved, to obtain solution a; then mixing the broken alcaine dibenzylin into solution a to obtain the solution b; putting the non-volatile high-boiling-point liquid at 4:1-6:1 volume percentage with the volatile solvent into the warm water at 25-35Deg. C, mixing and adding emulsion agent span-80 at 1-2% volume of high-boiling-point liquid, to obtain solution c; adding solution b into solution c; mixing for 5-7h in warm water at 25-35Deg. C, filtering, washing and drying. The invention can improve the drug function time and improve stability.
US20080031826 Devices containing lipid emulsions The present invention relates to compositions and methods for the storage and consumption of a lipid emulsion. In particular, the present invention relates to the storage of an omega-3 lipid emulsion for consumption in a container under non-oxidizing conditions.
CN103265593A Icariin derivatives The invention provides icariin derivatives disclosed as Formula I. The icariin derivatives provided by the invention have in-vitro acetylcholine ester inhibiting activity, and have better drug effects than icariin, thereby providing a new option for clinical medicines for treating senile dementia.
EP1140291B1 Combination chemotherapy comprising a mitotic inhibitor and a mek inhibitor Mitotic inhibitors such as paclitaxel have improved antitumor activity when used in combination with a selective MEK inhibitor, especially a phenyl amine compound of Formula (I) and (II).
US7070812 Process for producing dry powders of one or more carotenoids The invention relates to a process for producing dry powders of one or more carotenoids by a) dispersing one or more carotenoids in an aqueous molecular or colloidal solution of a mixture of lactose and a protective colloid and b) converting the dispersion which has formed into a dry powder by removing the water and, where appropriate, additionally used solvents and drying, where appropriate in the presence of a coating material, wherein at least one soybean protein is used as protective colloid in process step a).
CA2625974A1 Imidazole derivatives for the treatment of anxiety and related diseases This invention relates to imidazole derivatives V of formula (I), pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAAreceptor complex, and in particular for combating anxiety and related diseases.
CN101002796A Application of nanometer montmorillonite for pharmaceutical use, and medicine compositions therewith An application of the montmorillonite nanoparticles in preparing the medicine for treating the ulcer in digestive tract, regurgitation of stomach and esophagus, esophagitis, gastritis, colitis, acute diarrhea, chronic atrophic gastritis is disclosed. Its composite medicine is also disclosed.
US20120142622 Stambomycin and derivatives, their production and their use as drugs The present invention relates to Stambomycin compounds, their derivatives and their pharmaceutically acceptable salt thereof.
US20120071485 Therapeutic Compositions And Methods The present invention relates in general to therapeutic compositions and methods of use. In preferred embodiments, the invention relates to the field of eye health. In some embodiments, the invention relates to the prevention and treatment of macular degeneration by administering compounds disclosed herein. In some embodiments, the invention relates to compositions and methods of improving vision.
WO2005092328A1 Fxr activation compound A more potent therapeutic agent for hyperlipemia. It contains a compound having FXR activity and represented by the following formula (1) or (2).
CN103599068A Drug-loaded nano-micelle, anti-cancer medicament and preparation method thereof The invention provides a drug-loaded nano-micelle, an anti-cancer medicament and a preparation method thereof. The drug-loaded nano-micelle comprises hyaluronic acid and a chlorin e6 group which is connected on the straight chain of the hyaluronic acid through an adipic dihydrazide group, wherein the hyaluronic acid is used for coating the adipic dihydrazide group and the chlorin e6 group to form a core-shell structure, and the chlorin e6 group forms a hydrophobic inner core. The anti-cancer medicament is to load a hydrophobic anti-cancer medicament in the hydrophobic inner core of the drug-loaded nano-micelle. The drug-loaded nano-micelle has excellent biocompatibility, can be biodegraded and absorbed or excreted through a normal physiological manner, and has the functions of near infrared imaging and photodynamic therapy. According to the anti-cancer medicament, the hydrophobic anti-cancer medicament can smoothly reach a focus through the drug-loaded nano-micelle to realize an accurate sustained-release effect, so that the toxicity and immunogenicity can be reduced, and the half-time of body circulation of the anti-cancer medicament can be strengthened.
CN103370054A Lipid formulated compositions and methods for inhibiting expression of EG5 and VEGF genes This invention relates to compositions containing double- stranded ribonucleic acid (dsRNA) in a liquid particle formulation, methods of using the compositions to inhibit the expression of the Eg5/KSP and VEGF, and methods of using the compositions to treat pathological processes mediated by Eg5/KSP and VEGF expression, such as endometrial cancer.
US20100173940 Non-mucoadhesive film dosage forms Orally disintegrating film dosage forms for delivering active pharmaceutical agents, methods of formulating the dosage forms to retard absorption through the oral mucosa, and methods of using the dosage forms for the treatment of various medical conditions are provided.
CN102627603A Process of making crystalline aripiprazole The invention relates to a process of making crystalline aripiprazole, concretely crystalline aripiprazole Form B can be formed by crystallizing from a solvent selected from 1-propanol, 2-propanol, 1-butanol, ethyl acetate, acetonitrile or a combination thereof.
CN102813866A Medicine used for treating thermal bronchial asthma The invention relates to a medicine used for treating thermal bronchial asthma, relating to the technical field of medicines and solving the problem that most of existing Chinese patent medicines are used for full therapy and have poor pertinence. The medicine disclosed by the invention comprises the following components by weight: 10g of jute, 15g of semen armeniacae amarae, 10g of crude liquorice, 40g of plaster stone, 20g of fried cutellaria baicalensis, 15g of bamboo juice pinellia ternata, 15g of blackberry lily, 15g of semen lepidii, 50g of houttuynia cordata, 15g of radix stemonae, 20g of rhizoma anemarrhenae, 15g of earthworm, 15g of full fructus trichosanthis and 15g of sichuan fritillary bulb powder. The medicine disclosed by the invention can treat the thermal bronchial asthma and has the effects of clearing away heat and freeing lung and resolving sputum and relieving asthma.
WO2011029804A1 Inhibitors of jak The present invention relates to the use of novel compounds of Formula (I), (I) wherein the variables m, n, p, q, Q, r, R, R', X, X', Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
WO2008094969A2 Combination therapy with angiogenesis inhibitors Disclosed herein are methods of treating tumors using a combination therapy, wherein a VEGF antagonist and a protein kinase inhibitor capable of inhibiting at least the PDGF receptor tyronise kinase, are administered for a time and in amount sufficient to treat or prevent a tumor in a subject.
CA2286870C Indazole amide compounds as serotoninergic agents A compound having general formula (I) wherein R1, R2, R3, R'3, R4, R5 and R6 have the meanings stated in the description, acid addition salts thereof with pharmaceutically acceptable organic and inorganic acids and pharmaceutically acceptable quaternary salts thereof.
WO2005094811A1 Pharmaceutical product containing tranilast A pharmaceutical product comprising a package not only permitting viewing of its interior but also capable of inhibiting the decomposition of tranilast by light and, accommodated therein, a pharmaceutical preparation containing tranilast. The pharmaceutical product is produced by accommodating a pharmaceutical preparation containing tranilast and/or a salt thereof in a package permitting viewing of its interior, the package provided with light shielding means that blocks light of 350 to 450 nm wavelength region.
US20100286158 Dihydropyrimidinones This invention relates to dihydropyrimidinones of the formula wherein X and R1 to R7 are as defined in the description, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
WO2014060150A1 Cosmetic or dermatological preparation for prophylaxis and/or treatment of atopic dermatitis Agonists for the TRPM-8 receptor, more particularly one or more substances selected from the group consisting of, for example, linalool, geraniol, hydroxycitronellal, WS-3 (N-ethyl-p-menthane-3-carboxamide), WS-23 (2-isopropyl-N,2,3-trimethylbutyramide), Frescolat MAG (1,4-dioxaspiro[4.5]decane-2-methanol), Frescolat ML (menthyl lactate), Coolact P (5-methyl-2-prop-1-en-2-ylcyclohexan-1-ol) and Cooling Agent 10 (menthoxypropanediol), for use as medicaments to counter atopic dermatitis.
CN101301464A Candy for preventing influenza virus of children The invention relates to a candy for preventing children against influenza virus. Honeysuckle flower, forsythia fruit, dandehon herb, isatis root and ginger are made into a condensed extractum through a supercritical extraction method. The extractum is mixed with VC, lysine and kiwi powder evenly, then cooked syrup is put into a candy forming machine for forming and cutting, and the candy is prepared finally after sorting defectives, package and sterilization.
US20120213800 Methods for treating and diagnosing disease The present invention provides methods for the diagnosis and/or treatment of chronic kidney disease, immune complex-mediated GN, rheumatoid arthritis, and pulmonary fibrosis, and methods for identifying compounds for such therapeutic use.
WO2013022092A9 Heptamer-type small guide nucleic acid capable of inducing apoptosis of human hematologic cancer cells Provided are: a heptamer-type small guide (sg) nucleic acid which can induce the apoptosis of at least two types of human hematologic cancer cells and comprises any seven nucleotide sequences selected from SEQ ID NO: 1 to SEQ ID NO: 12; and a therapeutic agent for cancer, which contains the heptamer-type small guide nucleic acid as an active ingredient. A novel heptamer-type sg nucleic acid can be provided, which can induce the apoptosis of at least two types of hematologic cancer cells.
US20100286167 Dihydroxyphenyl isoindolylmethanones This invention provides methods for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma, which comprise administering to the mammal a compound, salt, hydrate, tautomer or N-oxide according to formula (I): and in particular, those of subgenus VIIa These compounds inhibit or modulate the activity of the heat shock protein Hsp90.
WO2011139752A3 Preparation of polypeptides and salts thereof The application relates to processes for preparing polypeptides. Also provided are processes for preparing glatiramer acetate.
US7276242 Fowl pox viral construct composed of a first nucleic acid molecule encoding HIV Gag and/or Pol or derivatives and a second nucleic acid molecule encoding gamma-interferon and derivatives, effective in inducing, enhancing or otherwise stimulating an immune response to Gag and/or Pol. The invention relates to a fowl pox virus encoding an HIV antigen (gag and/or pol) and a cytokine (γ-interferon).
US7005138 Intravaginal or rectal delivery of selected serotonin reuptake inhibitors (ssris); antidepressants, analgesics, treating psychological disorders, pre-menstrual dysphoric disorder and obsessive compulsive disorders Methods and compositions are disclosed for the intravaginal or rectal delivery of selected serotonin reuptake inhibitors (SSRIs) to the systemic circulation. Such methods and compositions are useful in the treatment of depression, migraine headaches, chronic pain, psychoactive substance abuse disorders, pre-menstrual dysphoric disorder (PMDD) and obsessive compulsive disorders. The compositions may be formulated for the immediate release or controlled release of SSRIs over an extended period of time. A preferred SSRI is fluoxetine.
EP2168958A1 Isoindole-Imide Compounds, Compositions And Uses Thereof The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potent inhibitors of the production of the TNF-α in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory, allergic, and autoimmune diseases.
US20050221460 Novel genetic products from ashbya gossypii, associated with the structure of the cell wall or the cytoskeleton The invention relates to novel polynucleotides from Ashbya gossypii; to oligonucleotides hybridizing therewith; to expression cassettes and vectors which comprise these polynucleotides; to microorganisms transformed therewith; to polypeptides encoded by these polynucleotides; and to the use of the novel polypeptides and polynucleotides as targets for modulating the properties of the cell wall or of the cytoskeleton and, in particular, improving vitamin B2 production in microorganisms of the genus Ashbya.
CN1830431A Preparation method of potassium magnesium aspartate freeze dried powder injection A freeze-dried powder injection of spartase for supplementing electrolyte and treating arrhythmia, myocarditis sequelae, congestive heart failure, myocardial infarction, etc is prepared through reaction between L-aminobutanedioic acid and magnesium oxide, ultrasonic treating, cold storage, ultrafiltration, adding the filtered liquid prepared from potassium hydroxide and mannitol, filling in containers in dark condition, freeze drying and sealing.
CN103570616A N'-straight chain alkylacyl o-pyridine hydrazide derivative, its preparation method, medicinal composition and use The invention relates to an N'-straight chain alkylacyl o-pyridine hydrazide derivative shown as formula I, its pharmaceutically acceptable salts, hydrates and solvates, a preparation method thereof, a composition containing one or more of the compounds, and the use of the compounds in the treatment of protein kinase related diseases like immune disorder and tumor diseases.
US20120035241 Use of inhibitors of plac8 activity for the modulation of adipogenesis The present invention concerns Plac8, a new target involved in adipogenesis modulation. Using a siRNA approach, the inventors demonstrated that decrease in Plac8 activity in preadipocytes and adipose tissue induces a decrease in adipogenesis. Thus, the present invention relates to modulators of Plac8 activity as well screening test for identification of modulators as of the activity of this target, and their use, especially in pharmaceutical composition, to modulate adipogenesis and thus treat obesity and related disorders.
CN102302488A Applications of compound aiming at CCL18 target in preparing breast cancer resistant medicaments The invention provides applications of a compound aiming at a CCL18 target in preparing breast cancer resistant medicaments. The compound is L-ascorbyl palmitate, and can act as a breast cancer resistant medicament aiming at the CCL18 target; and the structural formula of the compound is shown as the formula I. The invention also provides a breast cancer resistant medicament, and the medicament contains an effective amount of the compound with structural formula shown as the formula I. The invention provides the applications of L-ascorbyl palmitate compound which is shown in the formula I and aims at the CCL18 target in preparing breast cancer resistant medicaments, and provides a novel medicament for treating breast cancer.
EP1487402B1 Composition including a pigment assembly comprising a mica core The present invention relates to a composition including a pigment assembly comprising a mica core, wherein said composition is intended to be applied on the skin on a mammal in need thereof for the prevention of skin damages caused by exposure to ultraviolet radiation.
CN101497603B Benzimidazole derivative containing alkoxy alkanamine oxyl substituted pyridine The invention belongs to the technical field of medicines, and in particular relates to a benzimidazole derivative containing pyridine substituted by alcoxyl and alkanamine oxygroup as well as pharmaceutically acceptable salts or isomers thereof shown in a general formula (I), wherein R<1>, R<2>, R<3>, R<4>, R<5> and n are defined as the specification. The invention also relates to a method for preparing the compounds and a pharmaceutical composition containing the compounds, and application of the compounds to preparing the medicines for treating and/or preventing peptic ulcer.
CN100577655C Andrographolidi natrii bisulfis and preparation method thereof The present invention provides one kind of sodium bisulfite andrographolide, which is prepared through adding water solution of sodium bisulfite into alcohol solution of andrographolide, heating to reflux, recovering alcohol, cooling, extracting with chloroform for several times, filtering, vacuum concentrating the filtrate, crystallizing the concentrated solution, suction filtering, and vacuum drying the filter cake to obtain the white sodium bisulfite andrographolide addition compound. The sodium bisulfite andrographolide product has high purity, high stability, high curative effect and wide use.
WO2007115808A1 Arginine prodrugs with high therapeutic activity Esters of arginine (L- and/or D- enantiomers) with D-galactose useful as prodrugs are described, possessing a high capacity for penetrating cell membranes and the blood-brain barrier. The esters of the invention, once absorbed, gradually release arginine and ensure prolonged and high levels of the drug, generating a substantial and extended therapeutic response over time.
WO2009084737A1 Compound having activity to suppress degranulation and cytokine production and use thereof The present invention provides a compound represented by the formula (I): wherein L is an alkylene group;X is a bond, -O-, -S- or -CO-;Y is a bond, -NR3- or -CO-;Z is an organic group or OH;R1 and R2 are the same or different and each is an optionally substituted alkyl group, a halogen atom or a hydrogen atom; and R3 is an optionally substituted alkyl group or a hydrogen atom, or a salt thereof.
WO2011126401A1 1,3-dialkyl-benzimidazole halogenides as agents for treating multiple sclerosis The invention relates to the field of psychoneurology and, in particular, to agents for treating multiple sclerosis. Substances that exhibit high activity in the treatment of multiple sclerosis are proposed from the group consisting of 1,3-dialkyl-benzimidazole halogenide compounds of general formula (I), where R1, R2 = methyl (Met), ethyl (Et), propyl (Pro), and X- = F-, Сl-, Вr-, J-.
USRE42461 Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—; R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7; R1 and R3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR6, —O(CH2)1-10CON6R7, —(lower alkylene)COOR6 and —CH═CH—COOR6; R6, R7 and R8 are H, lower alkyl or aryl-substituted Ic R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.
WO2010057104A2 Pyridoindole modulators of nmda receptor and acetylcholinesterase The present invention relates to new pyridoindole modulators of NMDA receptors, AMPA receptors, and/or L-type calcium channels, and/or inhibitors of acetylcholinesterase, pharmaceutical compositions thereof, and methods of use thereof.
CN103006668A Compound tablet containing tamsulosin (slow-release) and finasteride (quick-release) and preparation method thereof The invention relates to a compound tablet containing tamsulosin (slow-release) and finasteride (quick-release) and a preparation method of the compound tablet, and belongs to the field of pharmaceutical formulations.
WO2014138484A1 Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE ABSTRACT OF THE DISCLOSURE The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: {INSERT STRUCTURE HERE} I wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
EP1052977A4 Treatment of chronic inflammatory disorders of the gastrointestinal tract The present disclosure relates to an oral formulation for treating gastrointestinal inflammation that includes an effective amount of budesonide suspended in an edible oil, typically a vegetable oil. A method for treating gastrointestinal inflammation in mammals is also described and includes orally administering a composition of this invention to a mammal. In one embodiment, an initial dosage is administered daily for about two to four weeks and the dosage is subsequently tapered, generally at about two week intervals, in response to a reduction in symptoms until a minimum dose that controls symptoms is achieved.
WO2011096196A1 Lsd1 for target genes of cancer therapy and diagnosis The present invention relates to the roles played by a LSD1 gene in carcinogenesis and features a method for treating or preventing cancer by administering a double-stranded molecule against the LSD1 gene or a composition, vector or cell containing such a double- stranded molecule. The present invention also features methods and kits for detecting or diagnosing cancer in a subject, using the over-expressed LSD1 gene. Also, disclosed are methods of screening for candidate substances for treating and preventing cancer or inhibiting cancer cell growth, using as an index their effect on the expression or activity of LSD1.
US20090155176 Compositions and methods for treatment of diabetic retinopathy The present invention provides compounds and methods for the treatment of diabetic retinopathy. In particular, LFA-1 antagonists are described herein to be used in the treatment of diabetic retinopathy. One aspect of the invention provides for diagnosis of diabetic retinopathy and administration of a LFA-1 antagonist, after the patient is diagnosed with diabetic retinopathy.
US20120263798 Body Aqua The invention provides an entire line of deliciously flavored bottled water beverages with each flavor offering comprised of vitamins, minerals and nutritional supplements for fortifying the body. A sugar free, carbohydrate free and low sodium formula, Body Aqua features natural flavoring and natural sweeteners such as Stevia™. The Body Aqua product line contains ten varieties, with each formula designed to target a specific area of the body and promote overall health.
US20060040979 3-Aryl-2-hydroxypropionic acid derivative I A novel 3-aryl-2-hydroxypropionic acid derivative, a process and intermediate for its manufacture, pharmaceutical preparations containing it and the use of the compound in clinical conditions associated with insulin resistance.
WO2010066075A1 The use of hylotelephin in preparing medicaments for treating hbeag positive chronic hepatitis b in human The use of hylotelephin of the following formula in preparing medicaments for treating HBeAg positive chronic hepatitis B in human.
WO2011047412A1 Tyrosine and l-dopa for reducing l-dopa incorporation into proteins The present invention relates to the field of therapy and prophylaxis of complications and/or conditions associated with dopamine deficiency and/or insufficiency, and compositions for the treatment or prevention of such complications and/or conditions e.g., compositions comprising L-dopa and tyrosine.
US20110281859 Novel heterocyclic compounds as metap-2 inhibitors Compounds of the formula I, in which D, X, Y, Z, R and R1 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
CN101301268A Composition of doxycycline hydrochloride injection for animals and preparation technique thereof The invention discloses a composition of animal doxycycline hydrochloride injection and a process for making the same, belonging to the animal medicine technical field. The injection consists of principal medicine, solvent, a doxycycline hydrochloride complexing agent and antioxidant, wherein metal ion (Mg<2+>) of higher content is used as the doxycycline hydrochloride complexing agent so as to remarkably increase the solubility and the pH value of the doxycycline hydrochloride and to reinforce the stability of the injection at the same time; above all, the toxicity and the tissue irritation of medicine are reduced after complexation. Dissolvant mixed by 2-pyrrolidone and propylene glycol or dimethyl acetamide is used as solvent so as to increase the stability of the injection; therefore, the injection can not be separated out and frozen under a low-temperature (4 DEG C) condition; moreover, concentrated hydrochloric acid and ethanolamine are used as pH regulator. The invention develops the high-content doxycycline hydrochloride injection for veterinary clinic, and the injection has advanced process, convenient use and remarkable curative effect.
EP2632435A1 Liposomal drug composition containing a polymeric guanidine derivative A liposomal drug composition comprising: a dimeric or polymeric guanidine derivative or a pharmaceutically acceptable salt thereof as drug substance, and a lipid modified by polyethylene glycole (PEG). The drug composition have cytostatic and antimicrobial activity.
US20090074889 Compositions and Methods for Treatment and Prevention of Osteoarthritis The present invention is in the fields of medicine, pharmaceuticals, neutraceuticals and rheumatology. In one aspect, the invention provides pharmaceutical compositions for the treatment and/or prevention of osteoarthritis in mammals, particularly humans, comprising sodium bicarbonate and calcium gluconate, and optionally comprising one or more additional components. The invention also provides methods of treating or preventing osteoarthritis by administering to a mammal, preferably via intraarticular injection, one or more compositions of the invention.
EP1797078A1 Compounds, compositions containing them, preparation thereof and uses thereof iii Compounds of Formula I, or pharmaceutically acceptable salts thereof: I (chemical formula to be inserted here - please see paper copy) wherein R1, R2, R3, R4, R5, R6 and G are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
CN101959878A Substituted oxindole-derivatives and the use thereof for the treatment of vasopressin-dependent illnesses The present invention relates to novel substituted oxindole-derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.
WO2011130877A1 Crystalline form of methylprednisolone aceponate monohydrate and preparation methods thereof A crystalline form of methylprednisolone aceponate monohydrate exhibits an X-ray powder diffraction pattern having characteristic peaks at the diffraction angles 2θ= of 8.6°, 12.2°, 13.6°, 15.3°, and 19.3°. The method for preparing the crystalline form comprises dissolving methylprednisolone aceponate in the mixture of water and organic solvent completely, and then evaporating the organic solvent. Another method comprises dissolving methylprednisolone aceponate in organic solvent completely, and then gradually adding water to precipitate the crystals of methylprednisolone aceponate monohydrate.
US20120004284 Pdk inhibitor compounds and methods of use thereof The invention relates to methods of treating or preventing acquired or congenital mitochondrial diseases or disorders, including treating cell proliferation related disorders or diseases, such as cancer. The invention further relates to pharmaceutical compositions for treating such disorders or diseases.
US7338941 Identifying a mammal; administering isovitexin or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof Methods of treating a mammal with high blood-glucose, or high blood-cholesterol, levels with isovitexin, and pharmaceutical compositions comprising the same are disclosed.
WO2010115342A1 SUSTAINED RELEASE COMPOSITION CONTAINING TETRAHYDROPYRIDO [4, 3-b] INDOLE DERIVATIVE AND PREPARATION METHOD OF DERIVATIVE A sustained release pharmaceutical composition containing dimebolin or pharmaceutical salt thereof as an active component, a preparation method for said pharmaceutical composition and a preparation method for said compound are provided. Said composition is suitable for oral administration, once a day, and reaches the peak plasma concentration within 1-3 hours after oral administration. The composition is useful for preparing medicament for treating cognitive disfunction syndrome, Alzheimer's disease, Parkinson's syndrome, Huntington's syndrome, and senile dementia.
CN102552315A Compound sodium chloride potassium chloride infusion solution The invention relates to the field of pharmacy, and specifically relates to a compound sodium chloride potassium chloride infusion solution. The invention solves a technical problem, and provides an electrolyte supplementing medicine which is an infusion solution prepared with sodium chloride and potassium chloride as active components. Every 100ml of the infusion solution contains 0.05-0.33g of potassium chloride and 0.7-1.1g of sodium chloride. The infusion solution is applied with an intravenous drip mode, and is used for severe hypokalemia patients or patients cannot be subject to oral administrations. Potassium supplementation dosages, concentrations and speeds are determined according to clinical pathogenetic conditions, blood-potassium concentrations and electrocardiogram potassium deficiency figures.
CN102309454A Preparation method of econazole nitrate/polyacrylic resin cationic nanoparticles The invention discloses a preparation method of econazole nitrate/polyacrylic resin nanoparticles. The preparation method comprises the steps of: dissolving polyether F-68 in a phosphate buffer solution to obtain an aqueous phase, dissolving econazole nitrate and polyacrylic resin RS100 in a mixed solution of acetone and ethanol to obtain an organic phase, adding the organic phase into the aqueous phase for reaction, then removing an organic solvent and unreacted F-68, then adding an osmotic pressure regulator, a bacteriostat and a buffer, and finally regulating a pH value to be 4.5-7.0. In the invention, a solvent-diffusion method is used for preparing econazole nitrate/RS100 nanoparticles, a vacuum volatilization method is combined with an ultrafiltration method to remove the organic solvent, buffer salt and a free surfactant, and a preservative, the osmotic pressure regulator and a thickener are added after volume metering to prepare an econazole nitrate/RS100 nanoparticle colloidal solution, which has the zeta potential ranging from +26mV to +35Mv, has stronger medicine carrying capacity and is particularly suitable for ocular surface medication.
CN101591337A Compound formed by splicing ferulic acid and matrine compound and application thereof The invention relates to a salt, amide or ester compound formed by splicing ferulic acid and a matrine compound and application thereof. The newly formed compound has the advantages of increasing the biological function of the matrine compound and/or the ferulic acid, reducing the toxicity of the matrine compound and/or the ferulic acid or increasing the solubility of medicaments.
US7381724 6(5-chloro-2-pyridyl-)-5-[4-methyl-1-piperazinyl]carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine for tranquilizers or hypnotics Dextrorotatory isomer of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, its preparation and pharmaceutical compositions containing it which are usable as tranquillisers and hypnotics.
US7109351 Fused pyrrolecarboxamides; GABA brain receptor ligands Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
WO2006062069A1 REMEDY FOR PRURITUS COMPRISING p38MAP KINASE AS THE ACTIVE INGREDIENT It is intended to find a novel pharmacological effect (a medicinal use) of a p38MAP kinase inhibitor. Because of having an excellent antipruritic effect, a p38MAP kinase inhibitor is useful as a remedy for pruritus of any types such as ocular pruritus, skin pruritus and general pruritus.
WO2008142147A1 Combination comprising pyrrolidone-5-carboxylic acid and at least one compound from citrulline, arginine and asparagine, and use thereof in the treatment of atopic dermatitis Combination comprising pyrrolidone-5-carboxylic acid and at least one compound from citrulline, arginine and asparagine, and use thereof in t he treatment of atopic dermatitis The present invention relates to a composition comprising, in a physiologically acceptable carrier, pyrrolidone-5-carboxylic acid and at least one compound from citrulline, arginine and asparagine, in racemic or isomer form, and salts t hereof, for the preparation of a medicament for use in the treatment and/or prevention of atopic dermatitis.
US20090227664 Expression Vectors Able to Elicit Improved Immune Response and Methods of Using Same The invention relates to nucleic acids (such as DNA immunization plasmids), encoding fusion proteins containing a destabilizing amino acid sequence attached to an amino acid sequence of interest, in which the immunogenicity of the amino acid sequence of interest is increased by the presence of the destabilizing amino acid sequence. The invention also relates to nucleic acids encoding secreted fusion proteins, such as those containing chemokines or cytokines, and an attached amino acid sequence of interest, in which the immunogenicity of the amino acid sequence of interest is increased as a result of being attached to the secretory sequence. The invention also relates methods of increasing the immunogenicity of the encoded proteins for use as vaccines or in gene therapy.
CN102416166B Aerosol inhalant containing interferon alpha and ipratropium bromide The invention belongs to the field of medicinal compositions for resisting virus, and relates to an aerosol inhalant containing interferon alpha and ipratropium bromide. The aerosol inhalant contains a therapeutically effective amount of interferon alpha, a therapeutically effective amount of ipratropium bromide and an appropriate amount of pharmaceutic auxiliary materials; preferably, single dose of the aerosol inhalant contains 2.5 to 30mu g of interferon alpha, 0.025 to 0.2mg of ipratropium bromide and an appropriate amount of pharmaceutic auxiliary materials; and more preferably, single dose of the aerosol inhalant contains 10 to 20mu g of interferon alpha, 0.05 to 0.1mg of ipratropium bromide and an appropriate amount of pharmaceutic auxiliary materials. Compared with the interferon alpha or the ipratropium bromide, the aerosol inhalant containing the interferon alpha and the ipratropium bromide has the advantages that the effect of treating viral pneumonia can be improved obviously.
US20080021100 Pharmaceutical Formulations and Compositions of a Selective Antagonist of Either CXCR2 or Both CXCR1 and CXCR2 and Methods of Using the Same for Treating Inflammatory Disorders The present invention provides compositions as well as kits and methods based on a selective antagonist of either CXCR2 or both CXCR1 and CXCR2 that are useful for treating inflammatory disorders.
US7645736 injecting an alpha-v. beta 3 or alpha-v, beta 5 inhibitor into the vitreous body of the eye; angiogenesis inhibition; diabetic retinopathy, macular degeneration, myopia, ocular histoplasmosis; (2S)-2-benzyloxycarboxamido-3-(2-guanidinomethyl-1,4-benzodioxan-6-yl)propionic acid Methods for the treatment of a disease of the eye of a patient comprising injecting into the vitreous body of the eye a composition comprising a therapeutically effective amount of an αvβ3 and/or αvβ5 inhibitor sufficient to inhibit angiogenesis and inhibit neovascularization in the treated eye. The αvβ3 and/or αvβ5 inhibitor being a compound of formula II: as defined herein or a physiologically acceptable salt thereof.
CN102488679A Application of sodium dodecyl benzene sulfonate in preparing externally applied medicaments for treating tinea manus and tinea pedis The invention provides application of sodium dodecyl benzene sulfonate in preparing externally applied medicaments for treating tinea manus and tinea pedis.
CN102525969A Hydroxychloroquine sulphate solid preparation and preparation method thereof The invention discloses a hydroxychloroquine sulphate solid preparation, which contains hydroxychloroquine sulphate or pharmaceutically acceptable salts thereof and an auxiliary material, wherein the auxiliary material comprises a buffer pair; the buffer pair is dissolved in water to form a buffer solution with pH of 4-6.5; and the content of the buffer pair is 0.05-2% in terms of mass percentage. The invention further discloses a preparation method of the hydroxychloroquine sulphate solid preparation. The hydroxychloroquine sulphate solid preparation disclosed by the invention has excellent dissolution property and stability, and particularly, is obviously increased in stability compared with the prior art.
US20060069154 Enzyme activated self-immolative n-substituted nitrogen mustard prodrugs This invention pertains to certain enzyme (CPG2) activated self-immolative nitrogen mustard prodrugs, which are useful in enzyme prodrug therapy (EPT), such as ADEPT and GDEPT, for the treatment of proliferative conditions, such as cancer, and which have the following formula: wherein: RN is independently C1-7alkyl; X1 is independently —I, —Br, or —Cl; X2 is independently —I, —Br, or —Cl; the group —N(CH2CH2X1)(CH2CH2X2) is independently attached at the 2-position or at the 4-position; each RG is independently —H or an ester substituent; n is independently an integer from 0 to 4; each RP, if present, is independently a phenyl substituent; m is independently an integer from 0 to 4; each RM, if present, is independently a mustard substituent; and pharmaceutically acceptable salts, solvates, amides, and esters thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds; such compounds and compositions for use in methods of treatment of the human or animal body by therapy; the use of such compounds and compositions for the manufacture of medicaments for the treatment of proliferative conditions; and the like.
CN101028254B Sustaining agent of Duosuo theosine and its preparation A slow-release doxofylline is composed of a fast-release component prepared from doxofylline (10-60%) and fast-release assistant and a slow-release component prepared from doxofylline (40-90%) and slow-release assistant. Its preparing process is also disclosed.
CN103040097A Apple scent type snuff The invention belongs to the technical field of snuff products and relates to apple scent type snuff made of all natural raw materials and a preparation method of the snuff. The snuff comprises, by weight, 100-500 parts of green tea leaves, 0.05-0.35 part of musk, 50-150 parts of lily magnolia, 10-90 parts of centipede minima, 100-300 parts of mulberry leaves, 0.1-0.4 part of borneol, 0.03-0.10 part of asarum, 0.01-0.09 part of rhinoceros horn, 5-15 parts of acorus tatarinowii, 25-125 parts of tobacco leaves, 2-6 parts of sandalwood, 2-6 parts of flos caryophyllata, 5-25 parts of radix angelicae dahuricae, 2-6 parts of menthol and 50-150 parts of red wine. The snuff is smoked by apples, has the faint scent of the apples, and is refreshing and capable of enabling a nasal cavity to ventilate and assisting smoking cessation.
CN101411711A Composition containing alisol A and alisol A 24-acetic ester and use The invention provides a composition consisting of alisol A and alisol A24-acetic ester and application thereof, wherein weight ratio of the composition consisting of the alisol A and the alisol A24-acetic ester is between 1: 0.02 and 1: 50. The invention provides a medicine for treating hyperlipidemia diseases, atherosclerosis diseases or fatty liver diseases by modern medical theory so as to satisfy needs for clinical application. The invention has the advantages that people taking the composition consisting of the alisol A and the alisol A24-acetic ester for a long time do not have abnormal rise of liver transaminase, intrahepatic fat deposit, or increase of liver volume and/or weight. The creativity of the invention lies in that through a systematically study of the specific mixture ratio of the alisol A and the alisol A24-acetic ester, the curative effect of decreasing blood-fat, resisting atherosclerosis and treating fatty liver can be improved, and toxic and side effect can be reduced.
CN103360240A Preparation method of high purity fenofibric acid The invention provides a preparation method of high purity fenofibric acid. The preparation method successively comprises the following steps: reacting to produce fenofibric acid; crudely purifying of the fenofibric acid to obtain a fenofibric acid crude product; and refining the fenofibric acid to obtain the high purity fenofibric acid. The high purity fenofibric acid prepared by the preparation method has a purity of more than 99.5%, and is safe and reliable.
WO2008039139A1 Novel 5,7-disubstituted [1, 3] thiazolo [4, 5] pyrimidin-2 (3h)-amine derivatives and their use in therapy There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.
US7173038 Treatment of diseases such as cancer or arthritis The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof, processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as a active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of number of disease states including cancer and rheumatoid arthritis.
DE20321314U1 Retarded release pharmaceutical composition, obtained without use of organic solvents or water by densifying mixture of active agent and retarding polymer in heated rollers Production of a retarded release pharmaceutical composition (A) involves: (a) forming a mixture of active agent (I) and release retarding polymer (II); (b) densifying the mixture by passage between two rollers at a temperature of more than 40 [deg]C under a force of 15-40 kN per cm of roller width; (c) comminuting the densified mixture to the required particle size; and (d) optionally further processing the mixture. An independent claim is included for the composition (A) obtained by the process. -
CN101766619B Pharmaceutical composition for malignancy treatment and application thereof The invention discloses a pharmaceutical composite for malignancy treatment and an application thereof. The pharmaceutical composite is proportionally prepared by curcumin and tetrandrine. The medicine prepared thereby comprises a preparation-allowed pharmaceutical excipient or carrier. The important point is that the synergistic effect of curcumin and tetrandrine on malignancy treatment is discovered. In particular, the pharmaceutical composite is applicable to glioma, lung cancer, liver cancer, gastric cancer, intestinal cancer, breast cancer, cervical cancer, pancreatic cancer and leukemia. The medicine has reasonable formulation, definite effective ingredients and obvious antitumor effect, and can reduce the clinical administration of the existing anticancer drugs, improve anticancer effect, reduce toxic side effect, and has application prospect of preparing antitumor drugs.
WO2008100547A3 Compositions comprising lamiridosin, iridoids or derivatives thereof for treatment of hepatitis c or hepatitis b The present invention comprises compositions and methods for the treatment of liver disease, particularly treatments for infection by HCV and/or HBV. The present invention comprises antiviral compositions comprising lamiridosin, derivatives of lamiridosin or iridoids that are effective in inhibiting one or more steps in the infection of cells by HCV or HBV. Methods for treating subjects, particularly humans, infected with HCV or HBV are provided.
WO2007015578A1 Method for assay on the effect of vascularization inhibitor Disclosed is a method for prediction of the effect of a vascularization inhibitor. The anti-tumor effect of a vascularization inhibitor can be predicted by evaluating the EGF-dependence property of the inhibitor with respect to the proliferation and/or survival of a tumor cell and using the evaluated EGF-dependence property as a measure. The anti-tumor effect of a vascularization inhibitor correlates with the EGF-dependency property of the inhibitor with respect to the proliferation and/or survival of a tumor cell. Therefore, a vascularization inhibitor can exert an excellent anti-tumor effect by using it in combination with a substance having an EGF inhibitory effect.
CN102366424A Dermatophytosis treatment powder The invention discloses dermatophytosis treatment powder, and belongs to the field of a medical science. The dermatophytosis treatment powder is a drug for treating dermatophytosis. The dermatophytosis treatment powder is an ancestral externally-applied drug, is prepared from realgar and alum, and can treat carbuncles. Results of multiple experiments show that the dermatophytosis treatment powder has excellent effects. The preparation and the use of the dermatophytosis treatment powder comprise the steps of grinding realgar and alum into fine powder, wherein use amounts of realgar and alum are same, mixing well the fine powder by edible vinegar, and smearing the mixture on an affected part of feed or immersing feet into the mixture.
CN102973653A Preparation method of tanshinone extract and water soluble substance thereof The invention provides a preparation method of a tanshinone extract and a water soluble substance thereof. The preparation method comprises the following steps of: extracting tanshinone by alcohol with the concentration being greater than or equal to 80%, wherein the tanshinone is segmented tanshinone or a complete material, and the mass ratio of the alcohol to the tanshinone is (5-20):1, heating and carrying out refluxing extraction for 2-5 times, combining and filtrating to obtain an extracting solution, wherein the extraction lasts for 0.25-3h every time; carrying out vacuum concentration on the extracting solution till an extract without the alcohol taste is obtained; and washing the extract by water for 5-12 times and drying under reduced pressure to obtain the tanshinone extract which contains 10.0-15.0% of tanshinone IIA and 8.0-11.0% of cryptotanshinone. The tanshinone extract prepared by the method provided by the invention has the advantages that the content of active substances is high, and the solubility of the water soluble substance of the tanshinone extract is good.
US20100099697 Method of Treatment Using Inhibitors of Mitosis Methods of treating diseases caused by cell division or that are treated by inhibiting mitosis by administering two doses of an inhibitor of mitosis between the biologically effective dose and the maximum tolerated dose in a dosing cycle that allows for the recovery or subsiding of side effects, wherein the second dose is administered 24 to 48 hours after the first dose.
US7495104 Quinoline or quinazoline derivatives inhibiting auto-phosphorylation of fibroblast growth factor receptors An objective of the present invention is to provide novel compounds which have inhibitory activity against autophosphorylation of an FGF receptor family and, when orally or intraveneously administered, can suppress the growth of cancer cells. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X represents CH or N; Z represents O or S; Q represents NR10, CR11R2, carbonyl, O, S(═O)m, wherein m is 0 to 2, or urea; R1 to R3 each independently represent H, OH, halogen, nitro, amino, alkyl, alkoxy or the like in which the alkyl and alkoxy groups are optionally substituted; R4 represents H; R5 to R8 each independently represent H, halogen, alkyl, or alkoxy; and R9 represents an optionally substituted carbocyclic or heterocyclic group.
CN101904835B Application of curcumin-zinc compound in preparing bacteriostatic analgesics or health care products The invention discloses application of a curcumin-zinc compound in preparing bacteriostatic analgesics. The invention discloses the curcumin-zinc compound has good bacteriostatic abirritation, can be used for curing common diseases of retinopathy, skin ulcer and the like caused by bacterial infection, pains and complications of diabetes and has effective treatment and wide application in curing various senile diseases. The curcumin-zinc compound can be used for preparing drugs and various health care products and solves the problems of single indication of the drugs and undesirable curative effect in curing the senile diseases at present. The curcumin-zinc compound has simple preparation method and wide application prospect.
CN1861605A Fleshy glossy ganoderma lactone A, preparation process and use thereof A Rouzhi lactone A is prepared from soft coral through extracting and separation. It can be used to prepare the anticancer medicines as it has high activity to suppress the activity of tumor cells.
US20070293501 Thioalkeneamides as Transketolase Inhibitors The present invention provides thioalkeneamides of formula (I) which are useful as transketolase inhibitors: wherein R1, R2, R3, R4, R5, R6, Ra-Rd, n and ring A are as defined herein. The present invention also provides pharmaceutical compositions comprising the compounds of formula (I). The invention provides methods for inhibiting transketolase activity, reducing cellular ribose-5-phosphate levels, inhibiting nucleic acid synthesis, inhibiting cell proliferation and tumor cell growth in vitro and in vivo, stimulating apoptosis in tumor cells and treating cancer by administering a compound of formula (I) or a pharmaceutical composition thereof.
CN101385703B Cation adhesion type natamycin nano eye drops A cationic adhesive-type natamycin nanometer eye drop comprises natamycin, a proper amount of osmoregulator and pH regulator. The eye drop is characterized by further comprising chitosan, pluronic F-68 and phospholipid, wherein, the mass percent concentration of the phospholipid in the eye drop is 0.01-2%, the mass percent concentration of the pluronic F-68 in the eye drop is 0.1-20%, and the masspercent concentration of the chitosan in the eye drop is 0.01-4%. The molecular weight of the chitosan is 5000-300000, and the deacetylation degree of the chitosan is greater than 85%. The natamycinnanometer eye drop is characterized by making a common natamycin suspension into suspension particles with the diameter ranging from 10nm to 1000nm, thus increasing solubility of the eye drop and enhancing safety and effectiveness. The natamycin particles of the common suspension are modified by the phospholipid and the chitosan to cause the particles to be positively charged, which is helpful toimprove absorption of the eye drop by cornea, enhances drug effect and prolongs the action time of the eye drop. And the chitosan has bioadhesion function, which enhances the adhesiveness between medicinal particles and the cornea.
CA2758302A1 Compounds and compositions comprising cdk inhibitors and methods for treatment of cancer Disclosed herein are compounds suitable for use as antitumor agents, methods for treating cancer wherein the disclosed compounds are used in making a medicament for the treatment of cancer, methods for treating a tumor comprising, administering to a subject a composition comprising one or more of the disclosed cytotoxic agents, and methods for preparing the disclosed antitumor agents.
US20100291099 Novel 27411, 23413, 22438, 23553, 25278, 26212, narc sc1, narc 10a, narc 1, narc 12, narc 13, narc17, narc 25, narc 3, narc 4, narc 7, narc 8, narc 11, narc 14a, narc 15, narc 16, narc 19, narc 20, narc 26, narc 27, narc 28, narc 30, narc 5, narc 6, narc 9, narc 10c, narc 8b, narc 9, narc2a, narc 16b, narc 1c, narc 1a, narc 25, 86604 and 32222 molecules and uses therefor The invention provides isolated nucleic acids molecules and proteins, designated 27411, 23413, 22438, 23553, 25278, 26212, NARC SC1, NARC 20A, NARC 1, NARC 12, NARC 13, NARC17, NARC 25, NARC 3, NARC 4, NARC 7, NARC 8, NARC 11, NARC 14A, NARC 15, NARC 16, NARC 19, NARC 20, NARC 26, NARC 27, NARC 28, NARC 30, NARC 5, NARC 6, NARC 9, NARC 10C, NARC 8B, NARC 9, NARC2A, NARC 16B, NARC 1C, NARC 1A, NARC 25, 86604 and 32222 nucleic acid molecules and proteins. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing said nucleic acid molecules, host cells into which the expression vectors have been introduced, nonhuman transgenic animals in which a said genes have been introduced or disrupted, fusion proteins, antigenic peptides and antibodies to said proteins. Diagnostic and therapeutic methods utilizing compositions of the invention are also provided.
WO2008111082A1 Process for the synthesis of ib-meca The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine; reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine); substitution of the halogen group with iodobenzylamine and removal of the diol protecting group.
CN102429604A Hand disinfecting wet tissue convenient to carry The invention discloses a hand disinfecting wet tissue convenient to carry, which consists of non-woven fabric and wet tissue liquor. The wet tissue liquor consists of glycerol, chlorhexidine gluconate, triclosan, ethanol, aloe extract, methylparaben, ethylene diamine tetraacetic acid, essence and purified water. The hand disinfecting wet tissue not only has a disinfecting performance, but also is added with skin care contents, and does not injure the skin of a user while disinfecting. The hand disinfecting wet tissue belongs to an alcohol-water system, is fresh, cool and not oily, is added with chlorhexidine gluconate and triclosan disinfecting contents, effectively kills bacteria of hands of the user, does not have any odor of disinfectant, is added with the skin care agent glycerol and the aloe extract, and effectively protects the skin of the user. Each package holds a piece of hand disinfecting wet tissue, the hand disinfecting wet tissue is clean and sanitary in use, is disposable, cannot be polluted even the wet tissue is used repeatedly, is easy to carry, and also can be used for disinfecting hands of workers in cosmetics and medicine production workshops.
WO2005077349A1 HUMAN β-DEFENSIN PRODUCTION ACCELERATOR A β-defensin production accelerator capable of accelerating the expression of human β-defensin. As an active ingredient of human β-defensin production accelerator, use is made of at least one component selected from the group consisting of an aloe vera extract, a gentian extract, a Rehmannias radix extract, a meadowsweet extract, an arnica extract, a gardenia extract, a peony extract, a carrot extract, an orange extract, a peach extract, a seaweed extract, a fermented soybean extract, levan, inulin, poly-D-glutamic acid, soybean fermentation bacteria, a fermentation product from rice extract, a wheat embryo extract, a wheat hydrolyzate, a soybean hydrolyzate, glycine, L-methionine, L-alanine, L-citrulline, propolis, polyphenol, a purine nucleic acid associated substance, lactoprotein, casein, a casein hydrolyzate, whey protein, a whey protein hydrolyzate, lactoperoxidase, lysozyme and lactoferrin. This human β-defensin production accelerator is provided as an external drug, cosmetic, food, internal drug, bath agent, etc.
WO2005096836A1 Sinapic acid supplementation An animal feed composition for monogastric non-human animals is disclosed comprising supplemental sinapic acid or derivatives thereof. Sinapic acid may be supplemented at a level of from 0.0005% to 3% of the feed composition by weight. The feed composition has the beneficial effect of promoting favourable intestinal microbial ecology by reducing pathogenic microbial populations, increasing favourable microbial populations, and increasing performance and growth characteristics in livestock animals.
EP2033959A1 Tetrahydropyranoquinoline derivatives 2-(Hetero)aryl-substituted 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydro-1,5-naphthyridine derivatives (I) (including tricyclic analogs, e.g. pyrano-quinolines), are new. 2-(Hetero)aryl-substituted 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydro-1,5-naphthyridine derivatives of formula (I) and their derivatives, solvates, tautomers, salts and stereoisomers (including mixtures in all proportions) are new. W = CH or N; R 1> - R 3> = H, R, A, Ar, halo, (CY 2) n-Q 1>, cycloalkyl, SMe, SCN, CF 3, OCF 3, OA, SCF 3, SF 5, SiMe 3, CO-(CY 2) n-Me, CH(CH 2) n-Q 2>, NCO, NCOOR, N(CH 2) nOH, CHNH 2, C(OH)R, CHNCOR, N(CH 2) nCOOR, N(CH 2) nCONR 2, XCONR(CH 2) nNR 2, N((CH 2) nXCOOR)-CO(CH 2) nAr, N((CH 2) nXR)-Q 3>, N((CH 2) nNRCOOR)CO(CH 2) nAr, N((CH 2) nNR 2)-Q 4>, O(CH 2) nNR 2, X(CH 2) nNR 2 or NCO(CH 2) nNR 2, or R 1> + R 2> = -N-C(CF 3)=N-, -N-CR=N- or -N-N=N-; Q 1> = SA, SCF 3, SCN, CF 3, OCF 3, OH, COOR, CN, halo, NR 2, OA, OCOA, CONR 2, NHCOA, NHSO 2A or N-pyrrolidone; Q 2> = NRCOOR, COOR, OH, NR 2, Ar, R 1> or X(CH 2) nAr; Q 3> = CO(CH 2) nAr, CO(CH 2) nXAr or SO 2(CH 2) nAr; Q 4> = CO(CH 2) nAr, CO(CH 2) nNRAr or SO 2(CH 2) nAr; Ar = aryl or heteroaryl; Y = H, A or halo; A = alkyl or cycloalkyl (both os by one or more halo); R = H or A, or geminal groups R = (CH 2) 5, (CH 2) 4, (CH 2) 2X(CH 2) 2 or (CH 2) 2Z(CH 2) 2; (MK#12) R 4>, R 5> = H, N-pyrrolidone residue (optionally substituted by one or more of OR, NO 2, halo, CF 3, OCF 3, CN, NR 2, SR or Ar), -X(CH 2) 2OR, -XCO(CH 2) nMe, -X(CH 2) 2NR 2, R 1>, arylthio, aryloxy or CH 2SiMe 3, or R 4> + R 5> = X(CR 2) 2, X(CR 2) 3, X(CHCH 2OR)(CH 2) 2, X(CHCH 2NR 2)(CH 2) 2, X(CH 2) 2NR 2, (CR 2) 3, X(CR 2) 4, CR=CR-CR=CR, XCHQ(CR 2) 2, XCHQCR 2, R-N-(C=X)-N-R or XC((CH 2) nOR) 2CH 2CH 2; X = O, S or NR; Q = halomethyl, CHO, COR a>, CH 2R a>, CH 2OCOR a>, CH 2NCOR 1>, CH 2N(R 1>) 2, CH 2OR 1>, CH 2OCON(R 1>) 2, CH 2OCOOR 1>, CH 2NHCON(R 1>) 2 or -CH 2NHCOOR 1>; R a> = -(CH 2) n-(X(CH 2) n) m-Q 5>, 4-(CH 2CH(CONH 2)-COO-(CH 2) nQ 6>)-1H-imidazol-1-yl, 2-oxa-3-oxo-4,7,7-tri-(R)- bicyclo-(2,2,1)-heptan-ylcarbonyloxy, OR, NHR 2, NR 2, NR(CH 2) n-aryl, NR(CH 2) n-OR, COOR, N-pyrrolidone, OCOR, NR(CH 2) n-NR 2, N((CH 2) nNR 2)CO(CH 2) nQ 7>, N((CH 2) nNHCOOR)-CO-aryl, R 1>, N(CH 2(CH 2) nOR) 2, NR(CH 2) nNCOOR, X(CH 2) nX(CH 2) nXR, X(CH 2) nX(CH 2) nOH, NR(CH 2) nO(CH 2) nOH, (CH 2) nCOOR, OCONR(CH 2) nOR, OCONR(CH 2) nNR 2, NR(CH 2) nNR 2, N((CH 2) nXR)CO(CH 2) nAr, N(R)(CH2) nN(R)COOR, XCOO(CH 2) nNR 2, OSO 2A, OSO 2CF 3, OSO 2-aryl, OCONR 2 or OCH 2(CH 2) nNR 2; Q 5> = 2- or 3-oxo-piperidino, 3,3,5,5- or 2,2,6,6-tetra-(R)-cyclohexyl or 3,3,5,5-tetra-(R)-piperidino, all having CH 2 in the 4-position replaced by Z, or R 1>-substituted 2-oxo-pyrrolidino, cyclopentyl, pyrrolidino (optionally substituted by NR 2 or in the 3-position by NA 2), R 1>-substituted 2-thienyl, 1H-imidazol-1-yl or 1H-1,2,4-tetrazol-1-yl; Q 6> = Ar or R 1>; Q 7> = CO(CH 2) nAr; Z = CH 2, X, CHCONH 2, CH(CH 2) n-Q 2>, NCO, NCOOR, N(CH 2) nOH, CHNH 2, C(OH)R, CHNCOR, N(CH 2) nCOOR, N(CH 2) nCONR 2, XCONR(CH 2) nNR 2, N((CH 2)XCOOR)-CO(CH 2) nAr, N((CH 2) nXR)-Q 3>, N((CH 2) nNRCOOR)CO(CH 2) nAr, N((CH 2) nNR 2)-Q 4>, O(CH 2) nNR 2, X(CH 2) nNR 2 or NCO(CH 2) nNR 2; R 6> = Ar (optionally substituted by one or more of Ar (optionally substituted by halo, NO 2, CN, A, OR, OCOR, COR, NR 2, CF 3 , OCF 3 or OCH(CF 3) 2), halo, NO 2, CN, OR, A, (CY 2) nOR, OCOR, (CY 2) n-COOR, (CY 2) n-CN, NCOR, COR or (CY 2) n-NR 2)); R 7> = COR, CONR 2, COOR, H or A; m = 0-2, and n = 0-7. Independent claims are also included for: (1) the preparation of (I); and (2) mixtures of compounds (I) with each other or with bis-aromatic compounds of formula (V) (specifically pentamidine or its salt) or their analogs or metabolites. Y', Z' = O or N; R 9>, R 10> = H, OH, halo, 1-10C alkoxy, OCF 3, NO 2 or NH 2; n = 2-6, and R 8>, R 11> (in m- or p-position) = -C(NH 2)=NH, -C(NH 2)=NOH, imidazolin-2-yl, 1-methyl-imidazolin-2-yl or tetrazol-5-yl. [Image] - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : Mitotic motor pr
US20100016298 Theramutein modulators This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
EP1282084B9 Method for preparing pyrimidone derivatives with antifungal activity The invention concerns a method for preparing pyrimidone derivatives of formula (I), characterized in that a compound of formula (II) is reacted with a compound of formula (III) in the presence of a base. Pyrimidone derivatives of formula (I) are useful as antifungal agents.
WO2010091067A3 Derivatives of [1, 3] oxazin- 2-one useful for the treatment of metabolic diseases such as lipid disorders This invention relates to novel compounds of an 11 β-HSD1 inhibitor disclosed herein, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11/3-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
WO2011085198A1 Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph) The invention generally relates to methods of treating a male subject with a prostate condition, for example, benign prostate hyperplasia (BPH). In certain embodiments, the invention provides methods of treating a male subject with a prostate condition, which include administering a MetAP2 inhibitor at a dose that does not substantially modulate angiogenesis.
US20120122958 Transcriptional repression leading to parkinson's disease Parkinson's disease is caused by the preferential loss of substantia nigra dopamine neurons. A Parkin Interacting Substrate, PARIS (ZNF746) is identified. The levels of PARIS are regulated by the ubiquitin proteasome system via binding to and ubiquitination by the E3 ubiquitin ligase, parkin. PARIS is a KRAB and zinc finger protein that accumulates in models of parkin inactivation and in human brain Parkinson's disease patients. PARIS represses the expression of the transcriptional co-activator, PGC-1α and the PGC-1α target gene, NRF-1 by binding to insulin response sequences in the PGC-1α promoter. Conditional knockout of parkin in adult animals leads to progressive loss of dopamine (DA) neurons that is PARIS dependent. Overexpression of PARIS causes selective loss of DA neurons in the substantia nigra, which is reversed by either parkin or PGC-1α co-expression. The identification of PARIS provides a molecular mechanism for neurodegeneration due to parkin inactivation.
CN102302520A Composition of chromium malate and bee glue and application thereof The invention relates to a composition of chromium malate and bee glue and application thereof, and belongs to the technical field of medicines. The composite contains the following components in part by weight: 17 to 102 parts of chromium malate and 500 to 3,000 parts of bee glue extract. The hyperglycemic effect of the composition of the chromium malate and the bee glue is more obvious than that of the single chromium malate or bee glue extract under the synergistic effect of the chromium malate and the bee glue extract. By tests of acute toxicity of mice, the composition does not have obvious toxic reaction, and reaches actual non-toxic level on the acute peroral toxicity of the mice. The composite can be widely applied to the treatment and prevention of diabetes, and can be prepared into medicaments or functional food of multiple formulations.
US20080064691 Heterocyclic Amide Derivatives Which Possess Glycogen Phosphorylase Inhibitory Activity A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; wherein, for example, Z is CH or nitrogen, R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from hydrogen, halo, nitro, cyano, hydroxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoromethoxy, carboxy and carbamoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; r is 1 or 2; R1 is halo, cyano or carboxy; Y is selected from —C(O)R2, —C(O)OR2, —C(O)NR2R3, -(1-4C)alkyl [optionally substituted] -(2-4C)alkenyl, —SO2NR2R3, and —S(O)cR2 (wherein c is 0, 1 or 2); R2 and R3 are independently selected from hydrogen, —O(1-4C)alkyl, —S(1-4C)alkyl, —N(1-4C)alkyl, heterocyclyl, aryl, and (1-4C)alkyl [optionally substituted]; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
EP1144385B1 Benzoheterocycles and their use as mek inhibitors The invention provides compounds having formula (I), wherein W is OH, or derivatives of the carboxylic acid, and Q is a heterocyclo-condensed ortho-phenylene residue. These compounds are useful as MEK inhibitors, particularly in the treatment of proliferative diseases such as cancer.
US20050053583 Method of inhibiting prion protein By inhibiting expression of a normal prion protein in prion-infected cells by using siRNA, it is possible to inhibit accumulation of an abnormal prion protein consequently. The inhibition of the abnormal prion protein accumulation can be applied in prevention and treatment of the prion diseases. This provides a method of inhibiting the abnormal prion protein accumulation. This method is applicable in preventing and treating the prion diseases whose effective method of treating has not been established at this moment. Further, use of this method is provided herein.
CA2266378C Use of sibutramine analogues to lower lipid levels A compound of formula (I) or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-(1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for lowering lipid levels and/or increasing the HDL : LDL cholesterol ratio in humans, for example in humans having hyperlipidaemia, hypercholesterolaemia or hypertriglyceridaemia.
WO2011103774A1 Pharmaceutical composition and use thereof in manufacturing medicaments for treating respiratory diseases Composition including a neutrophil elastase (NE)-targeting agent that counters the pathologic elements of respiratory inflammation is provided. NE-targeting agents primarily disrupt the association between NE and shed ectodomains of Syn-1, resulting in inhibition of the NE by protease inhibitors or anti-elastases. Non-anticoagulant heparin derivatives or fragments are exemplary NE-targeting agents. The composition preferably includes a carrier, such as chitosan or lactose in dry powder formulations, to facilitate delivery of the active agent. Use of the composition in manufacturing medicaments for treating respiratory diseases is also disclosed.
CN103705477A Tablets containing erlotinib hydrochloride and preparation method thereof The invention discloses erlotinib hydrochloride tablets which contain silica which accounts for 2-12 percent of the total weight of the erlotinib hydrochloride tablets. The dissolution can be promoted. The invention also relates to a method for preparing the tablets. The process flow is simple, special requirements on the granularity of the raw materials are avoided, and the dissolution property of the product is good.
US20080188508 Methods and Therapies for Potentiating a Therapeutic Action of an Opioid Receptor Agonist and Inhibiting and/or Reversing Tolerance to Opioid Receptor Agonists Combination therapies of an opioid receptor agonist and a cannabinoid receptor antagonist in an amount effective to potentiate a therapeutic activity of the opioid receptor agonist and/or inhibit, delay, reduce and/or reverse tolerance to the opioid receptor agonist are provided. Also provided are methods for use of these combination therapies in potentiating a therapeutic activity of an opioid receptor agonist and/or inhibiting, delaying or reducing development of acute and/or chronic tolerance to opioid receptor agonists and treating conditions treatable by opioid receptor agonist therapy in a subject. In addition, a method for reversing opioid receptor agonist tolerance and/or restoring therapeutic effect of an opioid receptor agonist in a subject via administration of a cannabinoid receptor antagonist is provided.
WO2011113370A1 Deuterium-substituted omega-diphenylurea and derivatives thereof and pharmaceutical compositions comprising these compounds The deuterium-substituted omega-diphenylurea, derivatives and pharmaceutically acceptable salts thereof are provided. The pharmaceutical compositions comprising the pharmaceutically acceptable carrier, the deuterium-substituted omega-diphenylurea and derivatives and pharmaceutically acceptable salts thereof are also provided. The deuterium-substituted diphenylurea can be used to treat or prevent cancer and other related diseases.
US20120238574 (1, 1, 1,3,3,3 -hexafluoro-2 hydroxypropan- 2 -yl) phenyl derivative, pharmaceutical compositions thereof and their use for the treatment of atherosclerosis The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.
WO2012106343A2 Hdac inhibitors and therapeutic methods using the same Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
CN203154592U Chinese and western medicine physical therapy belt for psoriasis The utility model relates to a Chinese and western medicine physical therapy belt for psoriasis, belonging to the field of medical instruments. The Chinese and western medicine physical therapy belt for psoriasis consists of a fixing strip 1, an electrothermal film 2, a medicine bag 3, a wire 4, a lithium battery 5 and a temperature controller 6, and is characterized in that the two ends of the fixing strip 1 are provided with nylon hasps 7, wherein the middle part of the fixing strip 1 is provided with the electrothermal film 2; the electrothermal film 2 is connected with the lithium battery 5 through the wire 4; the wire 4 is provided with the temperature controller 6; the inner side face of the electrothermal film 2 is provided with the medicine bag 3; the medicine bag 3 is made of sanitary breathable non-woven cotton fabric; and pharmaceutical ingredients in the medicine bag 3 comprise realgar, rhubarb, calomel, sulfur, lithargite, scorpion, centipede, fluocinonide ointment, erythromycin ointment and clotrimazole ointment. The Chinese and western medicine physical therapy belt has a simple structure and is convenient to use, the therapeutic effect of the medicines is improved by using the thermoosmosis effect of the electrothermal film, and the Chinese and western medicine physical therapy belt is an ideal Chinese and western medicine physical therapy belt for the psoriasis.
CN102247564A Liquid preparation for treating dermatitis, eczema and the like and preparation method thereof The invention discloses a liquid preparation for treating dermatitis, eczema and the like and a preparation technology thereof. The preparation is used for penetrating through the thickened layer of chronic and stubborn skin diseases to kill fungus and other pathogenic bacteria, and a corneum is softened to fall. The liquid preparation is composed of ethanol, propylene glycol, radix sophorae flavescentis, radix stemonae, Cortex Pseudolaricis, fructus cnidii, rheum officinale, goldthread root, benzoic acid, menthol, borneol, salicylic acid, Laurocapram, chlorhexidine acetate and methylparaben. The plant liquid of solid medicine is extracted by the ethanol, and then the obtained product is mixed with other components to obtain the liquid preparation for accelerating skin penetration, killing fungus and causing the stubborn skin diseases to recover.
US20060179496 Nucleic acid sequences differentially expressed in cancer tissue This invention relates to novel nucleic acid sequences which are differentially expressed in cancer cells. The invention also relates to proteins and peptides encoded by the sequences, to diagnostic assays and therapeutic agents based on the sequences and proteins, and to probes, antisense constructs, and antibodies derived from the sequences and proteins or peptides. The subject nucleic acids have been found to be differentially expressed by tumor cells, particularly in colon cancer tissue.
CN103351394A Acidamide substitution podophyllum derivative with antineoplastic activity and preparation method and application thereof The invention discloses an acidamide substitution podophyllum derivative with antineoplastic activity and a preparation method and application thereof. According to the invention, 2-pyrazine pyrazine, 5-methyl-2-pyrazine pyrazine, theophylline acetic acid and acetic acid are subjected to acidamide substitution reaction with 4'-demethylepipodophyllotoxin, so that the acidamide substitution podophyllum derivative with the antineoplastic activity, expressed by the formula (V), can be obtained. The acidamide substitution podophyllum derivative acts on cancer cells by means of multiple ways and multiple target points, and thus has better antineoplastic efficacy. As indicated by the in vitro cell activity inhibition test, the acidamide substitution podophyllum derivative disclosed by the invention has excellent antineoplastic activity and low toxic and side effects, and can be made into antineoplastic drugs for clinic antineoplastic treatment.
US20100047265 Active antiangiogenic therapy Application of oligonucleotide and polypeptide sequences of molecules of the family of the vascular permeability factor (VPF), their receptors, and co-receptors, as well as their modifications, in the active immunotherapy of pathologic entities in which course is associated to the increase of angiogenesis. These procedures can be employed in the single or combined therapy for the treatment of cancer and its metastasis, acute and chronic inflammatory processes, infectious diseases, autoimmune diseases, diabetic and newborn retinopathies, organ transplant rejection, macular degeneration, neovascular glaucoma, hemangioma, and angiofibroma, among others.
CA2157859C Amino acid-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent and a medicament containing them Benzoylguanidines of the formula I (see Formula I) in which the radicals R(1) to R(5) have the meanings given in the description, are described. They are prepared by reacting a compound of the formula II (see Formula II) in which R(1) to R(5) and L have the meanings given in the description, with guanidine. The compound I is suitable for the preparation of cardiovascular medicaments.
WO2007008563A3 Preparation of pegylated conjugates of vla-4 antagonists via a mitsunobu' s reaction Disclosed is a process for preparing polymer conjugates of agricultural, therapeutic, and food additive compounds using Mitsunobu conditions.
US20080221175 N-cyclohexyl benzamides and benzeneacetamides as inhibitors of 11-beta-hydroxysteroid dehydrogenases The present invention provides N-cyclohexyl benzamide and benzeneacetamide compounds according to formula (I): where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, m, n, p, and q are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11β-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.
US20110311516 Chemically Programmed Vaccination Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
CN101343274B Carbazoles alkaloid, preparation and application thereof The invention relates to a new carbazole alkaloid represented by the formula (1), and also relates to a preparation method thereof and applications thereof. The alkaloid is characterized in that: crude extracts of an organic solvent of Antipathes dichotcma (Pallas) are extracted with ethyl acetate or chloroform after being suspended on water, an ethyl acetate layer or a chloroform layer is collected for carrying out the normal pressure silica gel column chromatography, the thin-layer chromatography is used for tracing and combination, and a chloroform-acetone solvent system in a volume ratio of 9:1 is used for elution, the collected Rf value is about 0.5 to 0.7, and compositions of ultraviolet absorption exist under the wavelength of 254nm of an ultraviolet lamp, a crude product is gained, and a pure product is obtained through the further purification. The carbazole alkaloid can be used for preparing medicines treating gastric cancers, liver cancers and anti-herpes simplex virus, andhas the half inhibition concentration IC50 of 67.38mu g/mL and 73.65mu g/mL respectively to human gastric adenocarcinoma cell line SGC-7901 and human hepatoma cell Hep G2; and the IC50 value of the anti-herpes simplex HSV-I virus is 30.68mu g/mL.
US20110052567 Methods Compositions, Uses, and Kits Useful for Vitamin D Deficiency and Related Disorders Methods for diagnosing, treating, and preventing catabolism-related vitamin D deficiency and related disorders; related compositions, apparatus and kits, are disclosed. A method involves measuring CYP24 expression and/or activity, or a proxy thereof such as FGF23 level, in a patient and correlating abnormally elevated CYP24 expression and/or activity with catabolism-related vitamin D deficiency or with susceptibility for catabolism-related vitamin D deficiency. In response to abnormally elevated CYP24 expression and/or activity, the method further includes administering a CYP24 inhibitor to the vitamin D deficient or at-risk patient, and preferably avoiding activation of the vitamin D binding receptor, such as by avoiding administration of active vitamin D compounds to such patients. Optionally, a vitamin D prohormone or prohormone can be administered.
US7709020 Implantable device comprising phosphorus-containing macrolides This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which: A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M′ moiety may be saturated or unsaturated; each occurrence of x is independently an integer from 1-6; and the other variables are as defined herein.
CN1895253A Lomesaline hydrochloride eye drops and preparation thereof A kind of lomefloxacin hydrochloride eye drops is proportionally prepared from lomefloxacin hydrochloride and sodium hyaluronate through dissolving the lomefloxacin hydrochloride in water, adding the aqueous solution of sodium hyaluronate, stirring, adding water and loading in containers.
US20050222251 Dual inhibition of cyclooxygenase-2 and carbonic anhydrase Compounds of Formula I potently inhibit both cyclooxygenase-2 and carbonic anhydrases. Inhibition of carbonic anhydrases by a cyclooxygenase-2 inhibitor may affect significantly the safety and efficacy profiles of such a dual inhibitor in the treatment of cyclooxygenase-2 mediated disorders, compared to a cyclooxygenase-2 inhibitor without carbonic anhydrase inhibitory activity.
CN101095670A Luteolin phospholipid complexes and method for preparing the same and application thereof The invention relates to cyanidenon phosphatide compound, the preparation method and its applciaiton. The cyanidenon is gold yellow spicule that is separated from ethanol and contains one crystal water, it is slightly soluble in hot water, insoluble in cold water, and is not stable. So the biological utilization rate is low and medical effect is reduced and the parenteral administration is limited. The key is to increase its solubility, so the cyanidenon phosphatide compound is needed by market. The cyanidenon phosphatide compound comprises cyanidenon and phosphatide, with the weight proportion being 1: 0.2-25. The product can be used to prepare various dosage forms and combined with other active components.
WO2014097125A1 Pharmaceutical combination comprising binimetinib A combination of a CDK4/6 inhibitor and a MEK inhibitor for the treatment of diseases such as cancer.
US20080226649 Cytosine/guanine nucleotide sequences for use as therapeutic in treatment of allergy, asthma, cancer, infection, anemia, thrombocytopenia and neutropenia. Immunostimulatory compositions described as CpG-like nucleic acids are provided, including nucleic acids having immunostimulatory characteristics of CpG nucleic acid, despite certain substitutions of C, G, or C and G of the CpG dinucleotide. The substitutions can include, among others, exchange of methylated C for C, inosine for G, and ZpY for CpG, where Z is cytosine or dSpacer and Y is inosine, 2-aminopurine, nebularine, or dSpacer. Also provided are methods for inducing an immune response in a subject using the CpG-like nucleic acids. The methods are useful in the treatment of a subject that has or is at risk of developing an infectious disease, allergy, asthma, cancer, anemia, thrombocytopenia, or neutropenia.
CN1875947A An oral preparation containing caderofloxacin lactate The invention relates to a medicinal oral preparation containing Caderofloxacin lactate, wherein the active medicinal component being Caderofloxacin lactate, the medicinal auxiliary materials are selected from thinning agent, binding agent, lubricating agent, crumbling agent, antiadhesive, wetting agent. The obtained preparation comprises Caderofloxacin lactate 30-80%, thinning agent 1-60%, bonding agent 2-20%, lubricant 0.5-8%, crumbling agent 0-8%, antiadhesive 0-6% and right amount of wetting agent.
US20120232043 Lubiprostone for obstetrical or gynecological applications The invention relates to a method for terminating pregnancy or for menstrual induction, which method comprises administering a female subject with lubiprostone, preferably in combination of a progesterone receptor antagonist, such as mifepristone.
WO2005123136A1 Antiinflammatory and analgesic preparation for external use It is intended to provide an antiinflammatory and analgesic preparation for external use whereby side effects of a nonsteroidal antiinflammatory and analgesic drug on the skin can be regulated, the nonsteroidal antiinflammatory and analgesic drug can be prevented from degeneration with the passage of time due to a dibenzoylmethane derivative contained as an UV absorber therein, the dibenzoylmethane derivative can be prevented from crystallization and sedimentation due to an oily phase component contained therein, and the inherent effects of the nonsteroidal antiinflammatory and analgesic drug can be fully exerted without showing skin irritation caused by the oily phase component, an emulsifier and a thickener. The above problem can be solved by providing an antiinflammatory and analgesic preparation for external use which comprises a base for external use containing an oily component, a nonsteroidal antiinflammatory and analgesic drug and a dibenzoylmethane derivative and in which the total amount of fatty acid esters in the oily phase component is at least thrice as much as the content of the dibenzoylmethane derivative.
US20100022468 Nucleoside cyclic phosphoramidates for the treatment of rna-dependent rna viral infection The present invention provides nucleoside cyclic phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as pre-cursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside cyclic phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside cyclic phosphoramidates of the present invention.
WO2007099711A1 Differentiation inducer Disclosed is an inducer of the differentiation of a marrow cell into an endothelial cell. The inducer comprises heparin or a salt thereof as an active ingredient.
CN1657534A Penthorum seponin (PCPTS) and its antihepatitis and antimutation aetion A process for extracting and separating penthorum saponin (PCPTS) and its anti-hepatitis and anti-mutation actions are disclosed. It can be used for medicines and food.
US20120141412 Methods of treating idiopathic thrombocytopenic purpura with compositions comprising extracts of astragalus membranaceus The teachings provided herein generally relate to the preparation and uses of compositions comprising extracts of Astragalus membranaceus. The extracts are prepared from Astragalus membranaceus and can comprise, for example, an acid-modified arabinogalactan protein composition having an arabinose:galactose ratio ranging from about 3.5:1 to about 5.0:1, from about 5% to about 10% rhamnose, from about 15% to about 20% galactose, and from about 10% to about 15% glucose. The compositions can be used in the treatment of idiopathic thrombocytopenic purpura and the formulation of medicaments for such treatments.
US8178518 Mixture of androgen, macrocyclic ketone enhancer and thickener; glandular disorders A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.
CN101856345A Powder manufacturing method suitable for inhalation-type drug administration The invention relates to a powder manufacturing method capable of accurately controlling aerodynamic force size of power particles and is suitable for inhalation-type drug administration. In the method, after 3,6-double (4-double fumaryl aminobutyl)-2,5-diketopiperazine or salt substituent thereof is dissolved into alkaline solution, drug is directly added into the solution, or the alkaline solution and the acid solution are mixed under high shearing environment to form injectable suspension, and then drug is added; and the solution or the injectable suspension is dried to prepare drug particles suitable for aerodynamic force size (0.5-10 micrometers). The drug particles are transported to positions, such as patient nasal cavity, bronchus, lungs and the like by a dry powder inhaler; the characteristics that drug particles are quickly dissolved in human body environment with the pH value of 6.4-8 and drug particles are stable when pH value is less than or equal to 6.4 or more than 8 are utilized to realize quick and effective adsorption of drug.
CN103120656A Danshinolic acid A tablet and application thereof for preparing medicines The invention relates to a danshinolic acid A tablet which comprises a danshinolic acid A-containing composition, a filler, a disintegrating agent and a lubricant. The tablet comprises the following components in percentage by weight: 5-60% of danshinolic acid composition A, 90-35% of filler, 2-10% of disintegrating agent and 0.1-0.5% of lubricant. The content of danshinolic acid A in the danshinolic acid A-containing composition is greater than 93%, less than 100%. The tablet further comprises another four components: 0.1-2% of alkannic acid, 0.1-2% of rosmarinic acid, 0.1-2% of danshinolic acid B and 0.1-2% of danshinolic acid C. The filler is one or more of starch, dextrin, cane sugar, mannitol, microcrystalline cellulose, pregelatinized starch and calcium sulfate. The disintegrating agent is any one or more of carboxymethyl starch sodium, pregelatinized starch, crosslinked polyvinylpyrrolidone, low-substituted hydroxy propyl cellulose and crosslinked sodium carboxymethylcellulose. The lubricant is any one or more of magnesium stearate, talcum powder, superfine silica powder and superfine silica powder. The invention further discloses application of the danshinolic acid A tablet for preparing medicines for preventing and/or treating ischemic cerebrovascular diseases.
WO2014012511A1 N-(3-heteroarylaryl)-4-arylarylcarboxamtdes and analogs as hedgehog pathway inhibitors and use thereof Disclosed are novel N-(3-heteroarylaryl)-4-arylarylcarboxamides and analogs thereof, represented by the Formula I: wherein C cyclic group, D1-D4, Q1, Q2, R5 are defined herein. Compounds having Formula (I) are hedgehog pathway inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of hedgehog activity, such as cancer.
US20120122991 Method for treating cancer by increasing amp-activated kinase activity The invention relates to modulation of LKB1 or AMP kinase protein activity for treating disorders including diabetes and cancer. The invention also relates to screening for agents that modulate the activity of LKB1 or AMP kinase protein, which are useful in the treatment of diabetes and cancer, as well as preparing compounds for treatment of diabetes and cancer.
CN103169665A Oxaliplatin chitosan nanoparticle and application thereof The invention discloses an oxaliplatin chitosan nanoparticle and an application thereof. The preparation materials of the oxaliplatin chitosan nanoparticle comprise oxaliplatin, chitosan, sodium tripolyphosphate and an acetic acid aqueous solution. The oxaliplatin chitosan nanoparticle disclosed by the invention can be applied to preparing a drug for treating gastrointestinal tumors. Compared with the prior art, the oxaliplatin chitosan nanoparticle disclosed by the invention is small in grain size, high in encapsulation efficiency, low in material price and simpler in process.
WO2012053010A2 Method for treatment of acne using pharmaceutical compositions of clindamycin The present invention relates to a method for treating, reducing or preventing acne. In particular, the present invention relates to methods for reducing the total number, incidence and severity of acne lesions on the skin which includes both inflammatory and non-inflammatory lesions. Further, the invention relates to reducing the incidence and severity of adverse events resulting from topical application of anti- acne agents resulting in improvement of skin tone. The method includes administering a novel and stable topical anti-acne pharmaceutical composition.
US6864249 Pharmaceutical compositions containing them are of the class of thrombin inhibitors which are useful as anticoagulants. The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the class of thrombin inhibitors which are useful as anticoagulants.
CN101229168A Immunity excitant containing selenium The invention relates to an immune agonist containing element selenium for improving the immune function, in particular to a purine compound 8-substituted derivative. The immune agonist containing selenium element of the invention is a compound showed in formula (1). Owing to the immune-competence of the selenium element, the immune agonist containing selenium element of the invention leads to stronger immune improving activity of the compound than the corresponding compound analog (the representative compound 9) of the invention, which is applied in resisting viral diseases such as Hepatitis B Virus and Hepatitis C Virus, AIDS, SARS, human influenza and bird flu, and the treatment and assistance of various cancers, with good efficacy.
US20120101107 Piperazine dithioctate and pharmaceutical composition comprising the same The present invention relates to piperazine dithioctate, a novel addition salt of thioctic acid with a base and a pharmaceutical composition comprising the same. The piperazine dithioctate according to the present invention has good thermal and moisture stability and high water-solubility as well as dosage increase lower than other addition salts, thereby being effectively used for preparing a pharmaceutical composition for antioxidation or for preventing or treating diabetic polyneuropathy, etc.
CN103338754A Highly stable compositions of orally active nucleotide analogues or orally active nucleotide analogue prodrugs Disclosed are highly stable compositions having outstanding storage stability and/or demonstrating exceptional resistance to aqueous degradation, the composition including an orally active nucleotide analogue or an orally active nucleotide analogue prodrug, which is orally bioavailable, such as adefovir dipivoxil and tenofovir disoproxil. In particular molecular dispersions of adefovir dipivoxil in copovidone are disclosed. For example, when a composition of the invention is stored for 1 month or for 18 months at 25 DEG C and 60% relative humidity, its orally active nucleotide analogue or orally active nucleotide analogue prodrug degrades to provide a composition containing no more than 0. 2% or no more than 0. 7% by weight of a less orally bioavailable impurity, respectively. Also disclosed are a container/closure package system including the composition and a package insert and methods of manufacturing the composition and treating a patient for a disease or condition, for example, a viral disease or cancer, with the use of the composition.
CN1594306A Genistein-3'-sodium sulfonate, dimethylation daidzein-3'-sodium sulfonate, their preparing process and pharmaceutical use The invention provides a genistein-3'-sodium sulfonate, dimethylation daidzein-3'-sodium sulfonate and their preparing process comprising the steps of, charging reactants genistein or dismethylation daidzein into the dissolvent, charging sulphonating agent, subjecting the reactant and sulphonating agent to chemical reaction, separating the mixture by means of the conventional methods and purifying. The invention also provides a medicament and composition for treating cardiovascular and cerebrovascular diseases.
EP1946759A1 Therapeutic agent for nausea and/or vomiting A therapeutic and/or prophylactic agent for nausea and/or vomiting is provided. A therapeutic and/or prophylactic agent for nausea and/or vomiting, comprising a compound of the Formula (I) or a pharmaceutically acceptable salt or solvate thereof: (wherein R1 and R2 are each independently hydrogen or lower alkyl; R3 is hydrogen or lower alkoxycarbonyl; and R4 is hydrogen or lower alkyl; with the proviso that all of R1 to R3 are not simultaneously hydrogen; and R1 and R4 are not simultaneously hydrogen).
CN1977886B Medicinal composition of oxymatrine, ganoderma lucidum and astragalus The present invention discloses a new medicine composition and its preparation method. Said medicine composition is formed from (by weight portion) 100-1600 portions of kurarinone, 500-24000 portionsof ganoderma and 1000-80000 portions of astragalus root. Besides, it also can be made up by using 100-1600 portions of kurarinone, 2.5-700 portions of ganoderma polysaccharide and 5-1600 portions of astragalus polysaccharide. Said medicine composition can be made into various dosage forms, can be used for preparing the medicines capable or curing acute and chronic hepatitides and active hepatocirrhosis, etc.
CN1871013A Benzazepine derivatives as MAO-B inhibitors The present invention relates to novel benzazepine derivatives of the following formula: (I) wherein R<1>, R<2>, R<3>, R<4> and R<5>, X, X', Y and Y' are as defined in the description and claims, processes for their preparation, pharmaceutical compositions containing said derivatives and their use for the preparation of medicaments useful for the prevention and treatment of diseases in which selective inhibition of monoamine oxidase B activity plays a role or is implicated.
CN101766594A Officinal composition for lowering blood fat The invention discloses an officinal composition for lowering blood fat. Active ingredients are atorvastatin and probucol. The invention provides a better fat regulating drug for patients clinically suffering from severe lipid metabolism disorders and especially has favorable synergistic effect on patients at high liver function damaging risk level by drug combination; two kinds of drugs complement advantages so as to obviously lower the possibility of side effect occurrence because of increased amount of atorvastatin. The officinal composition for lowering blood fat is prepared from active ingredients and pharmaceutically acceptable supplementary materials, but is not limited in preparations, such as tablets, dispersible tablets, sustained release tablets and the like.
US20110082150 Headache pre-emption by dihydroergotamine treatment during headache Precursor events Disclosed are methods that address providing a subject experiencing, or who has experienced, a headache precursor event and administering dihydroergotamine, or a pharmaceutically acceptable salt or complex thereof, to the subject by oral inhalation, in an amount effective to pre-empt a subsequent headache in the subject. Also disclosed are compositions that are related to those methods.
CA2366865C Flupirtine in the treatment of fibromyalgia and related conditions The present invention is directed to a method for treating the symptoms associated with fibromyalgia and related conditions by administering flupirtine.
CN101601669B United medicine used for treating tumors The invention discloses a united medicine used for treating tumors, comprising manganoporphyrin, sodium cromoglyate and one or a plurality of optional medicinal carriers, or comprising the manganoporphyrin, dichloroacetic acid or pharmaceutically acceptable salt thereof and one or a plurality of optional medicinal carriers, or comprising the manganoporphyrin, any anti-tumor medicine and one or a plurality of optional medicinal carriers. The inventor of the application carries out a series of relevant experimental researches; and the experiments prove that by uniting the manganoporphyrin and the medicines which can be united for use as the medicine, the curative effect of the tumors can be enhanced, the toxicity of the medicine can be reduced, the survival time of experimental animals is prolonged, and an unlooked-for effect is obtained.
CA2748813A1 Pro-neurogenic compounds This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protectiong from neuron cell death.
US20050100534 firoin and firoin-A from extremophilic microorganisms ; active protection and stabilization of skin cells and their organic constituents (proteins, enzymes, membranes, nucleic acids or antioxidants); against damaging environmental influences, UV radiation. The invention relates to the incorporation of the low-molecular substance (compatible solute) β-mannosylglycerate (firoin) extracted from extremophilic microorganisms and/or of derivatives of this compound, e.g. an acid, a salt or ester, in particular, also of the β-mannosylglyceramide (firoin-A) in cosmetic or dermatological formulations for protecting skin from environmental influences and for improving the regenerability of the skin. Firoins (β-mannosylglycerate and β-mannosylglyceramide) are, according to the invention, involved in the active cell protection of the cell-specific free-radical scavengers, of the proteins, of the antioxidants, of the DNA, of the cell membranes and of other cell constituents by virtue of the fact that they protect (thermally, chemically and physically) these against damaging environmental influences, e.g. UV radiation, IR radiation and environmental stress. For other active substances added to the cosmetic formulation, firoins can serve as co-solvents and penetration intensifiers in order to not only stabilize these in the cosmetic formulation but also to actively transport them into deeper skin layers.
CN101679437A cyclopropyl fused indolobenzazepine hcv ns5b inhibitors The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Formula (I).
CN102210668B Application of cantharidin and derivants thereof in preparation of tumor chemotherapy sensitivity enhancing medicine The invention discloses application of cantharidin and derivants thereof in preparation of a tumor chemotherapy sensitivity enhancing medicine for enhancing sensitivity of tumors to treatment medicines. Both a compound and derivants thereof related by the invention have the functions of reducing MDR (Multiple Medicament Resistance) genetic transcription and expression in various tumor cells and further inhibiting occurrence of MDR, so that relatively strong tumor chemotherapy sensitivity enhancing function is displayed.
US20100298364 salts 756 The invention provides salts of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate, pharmaceutical compositions containing them and their use in therapy.
WO2013160896A1 Pomegranate oil for preventing and treating neurodegenerative diseases The present invention relates to the use of pomegranate oil and fractions thereof for preventing and treating neurodegenerative diseases. Particularly, the present invention relates to emulsions of the pomegranate oil or fractions thereof for the prevention and treatment of brain diseases, including Creutzfeldt-Jacob disease (CJD) and multiple sclerosis (MS).
WO2009149436A1 Substituted aminothiazole prodrugs of compounds with anti-hcv activity The invention provides amino-substituted aminothiazole compounds of Formula (I) and Formula (II) where A is a group of the formula: and the variables X, Y, R, and R1 to R7 are described herein. These compounds are prodrugs of compounds useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.
WO2007139887A3 Methods for treating bone or joint inflammation The present invention provides methods for promoting bone and joint health with certain compositions described herein or with optionally enriched extracts of plant material comprising such compositions. The present invention provides methods for the treatment or regulation of, bone and joint conditions such as joint inflammation, joint swelling, joint pain, gout, childhood arthritis, lupus arthritis, rheumatoid arthritis, and osteoarthritis.
EP2558081A2 Intraocular pressure reduction with intracameral bimatoprost implants The present invention provides a method of treating an ocular condition in an eye of a patient, comprising the step of placing a biodegradable intraocular implant in an eye of the patient, the implant comprising a prostamide and a biodegradable polymer matrix that releases drug at a rate effective to sustain release of an amount of the prostamide from the implant to provide an amount of the prostamide effective to prevent or reduce a symptom of an ocular condition of the eye, wherein said ocular condition is elevated IOP and said implant is placed in an intracameral location to dilate the outflow channels of the eye emanating from Schlemm's Canal.
CN1965857A Eye drop of povidone iodine and preparation process thereof The invention relates to a polyketone iodine eyedrops, and relative production, wherein it adds polyketone iodine into osmotic pressure adjuster, stabilizer, and pH adjuster to be dissolved, and using pH adjuster to realize constant volume; pH adjuster at 100 volume units contain 0.1-0.5 units of polyketone iodine, 0.35-0.65 osmotic pressure adjuster mass units, stabilizer at 0.05 mass units; the pH of osmotic pressure adjuster is 6.0-6.8. The invention can treat kinds of ceratitis, with high safety but no side effect.
US20110160263 Small molecule inhibition of PDZ-domain interaction Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula (I) or (III). The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds. Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl), inhibiting Wnt signaling.
WO2013073827A1 Composition containing natural minerals and the water extracted therefrom as active ingredients The present invention relates to a pharmaceutical composition for the prevention and treatment of diabetes, which contains natural minerals and the water extracted therefrom as active ingredients. More particularly, at least one mineral selected from the group consisting of lizardite, antigorite, brucite, magnesite, dolomite, talc, clinochlore, calcite, hornblende, and phologopite, and water which is extracted from the minerals and the quality of which is suitable for the standards of drinking water, contain a significantly large amount of rare earth elements, generate a large amount of far-infrared radiation and anions to enhance and promote health, block various forms of harmful radiation such as water vein waves and electromagnetic waves, stimulate the activity of the metabolism, and have the effects of remarkably inhibiting and reducing blood glucose for type 1 and type 2 diabetes. Therefore, the mineral and the water extracted therefrom can be effectively used in developing: a pharmaceutical composition for the purpose of preventing and treating diabetes, and a healthy food composition having the same purpose; a pharmaceutical composition for the purpose of preventing and treating cancer due to having the remarkable effects of inhibiting tumors from growing or metastasizing in the case of leukemia, colorectal cancer, stomach cancer, lung cancer, and skin cancer, and a healthy food composition having the same purpose; and a pharmaceutical composition for antibacterial purposes due to having highly antibacterial effects against colon bacillus and pseudomonas aeruginosa, as well as a composition to be externally applied to the skin and a cosmetic composition having the same purpose.
EP1606021A1 Manganese based organometallic complexes, pharmaceutical compositions and dietetic products The invention relates to compounds and their uses, particularly in the pharmaceutical and dietetic industries. The invention discloses complexes having Mn-SOD like activities, as well as methods for treating various diseases associated with oxidative stress, including cancer and inflammatory conditions, by administering said compounds. It further deals with pharmaceutical compositions or dietetic products comprising said compounds, more particularly useful to treat various diseases or disorders, in particular useful in the prevention or treatment of a disease involving an oxidative stress.
CN102525974A Meloxicam tablets for dogs and cats and preparation method for meloxicam tablets The invention relates to the field of medicine, and discloses meloxicam tablets for dogs and cats and a preparation method for the meloxicam tablets. The preparation method mainly comprises: a mixing step, a granulation step, a drying step, a granulation straightening step, a granule mixing step and a tabletting step. The meloxicam tablets consist of the following components in percentage by mass: 0.1 to 0.6 percent of meloxicam, 50 to 70 percent of lactose, 20 to 40 percent of microcrystalline cellulose, 3 to 5 percent of hydroxypropyl cellulose, 0.4 to 0.6 percent of sodium citrate, 1 to 5 percent of cross-linked polyvinylpyrrolidone, 4 to 8 percent of polyvinylpyrrolidone (PVP) K30, 0.2 to 0.8 percent of aspartame and 0.60 to 2 percent of magnesium stearate. The meloxicam tablets have small irritation on the intestines and stomach of the dogs and the cats, and are favorable for the absorption of active ingredients.
CN101292735A Sorbitol buccal tablet composition and preparing method thereof The invention relates to the composition of sopbitol buccal tablets and a production method thereof, which pertains to the field of foods, medicines and health care products. In addition, sopbitol coating technique can be applied to coating some medicines at will. The composition mainly comprises the sopbitol, binder, excipient and additive and is characterized in that the binder is one or the combination of sopbitol, acacia, sodium carboxymethylcellulose or starch; the sopbitol is adopted as a coating agent.
EP2544684A1 4,4-disubstituted piperidine derivatives useful as inhibitors of dipeptidyl peptidase-1 (dpp-1) The present invention is directed to 4,4-dl-substjtuted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
WO2006087544A3 Pyrrole derivatives as dna gyrase and topoisomerase inhibitors Compounds of formula (I) and their pharmaceutically acceptable salts are described: formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
US20110262373 Personalised pharmaceutical composition containing retinoic acid, for anti-aging of the skin The invention relates to a personalised pharmaceutical composition for anti-aging of the skin, in the form of an ointment, comprising a first group of common active principles present in any formulation, formed by retinoic acid, at least one anti-inflammatory agent, at least one additional depigmenting agent, at least one anti-oxidant and at least one vitamin; and a second group of variable active principles present in variable quantities formulated according to the metabolic characteristics of the particular user. The anti-inflammatory agent is indomethacin. The depigmenting agents can be selected from the group consisting of hydroquinone, kojic acid, mequinol, phytic acid and alpha-arbutin. The anti-oxidants can be selected from the group consisting of lipoic acid, lycopene, coenzyme Q10, resveratrol, pycnogenol®, L-carnosine, taurine, N-acetylglucosamine, ascorbic acid, isoflavones and tocotrienol. The second group of variable active principles can comprise hyaluronic acid, aloe vera, bilberry glycolic extract, centella glycolic extract, allantoin, organic silicon, niacinamide and a cicatrizant.
CN102531878A Novel crystal form of sodium valproate, and preparation method and application thereof The invention discloses a crystal form I of sodium valproate. In an X-ray powder diffraction pattern of the crystal, characteristic absorption peaks appear when a diffraction angle (2 theta) is equal to 5.54+/-0.1 degrees, 6.64+/-0.1 degrees, 20.90+/-0.1 degrees, 24.38+/-0.1 degrees and 26.13+/-0.1 degrees. The invention also discloses a preparation method and application of the crystal form I. According to the crystal form I of the sodium valproate, the moisture absorption is obviously reduced, low water content of the product is ensured, and the sodium valproate has stable quality in a storage period; when the moisture absorption is reduced, the dissolution time of the product is obviously shortened, the resolubility of the product is improved, the treatment effect and high safety of the sodium valproate in clinical treatment are ensured due to high resolubility, the pain during injection is relieved, the compliance of the patient in a treatment period is improved, and a good clinical effect is achieved.
US20120258087 Isotonic beverage with chelates The subject of the invention is an isotonic beverage with chelates containing carbohydrates, mineral amino acid chelates, L-carnitine, sweeteners, flavouring substances, and a diluent, the essential feature of the beverage being the content of up to 0.1 wt % of mineral components in the form of mineral amino acid chelates, preferably bisglycinates and glycinates, from 0.1 to 50 wt % of isomaltulose, up to 15 wt % of L-carnitine and/or its derivatives, from 5 to 84% of carbohydrates, up to 50 wt % of bioactive substances, up to 50 wt % of flavouring substances, up to 80 wt % of polyalcohols, diluents, tableting aids, stabilizers, antioxidants, dyes, and 0.013-25 wt % of sweeteners, whereby its osmolarity is 275-295 mOsm/kg and pH is 2-5.
US7268157 Substituted arylalcanoic acid derivatives as PPAR pan agonists with potent antihyperglycemic and antihyperlipidemic activity Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.
CN101704874A Pentacyclic triterpene and melbine salt of derivative thereof, preparation method and medical application of pentacyclic triterpene The invention relates to field of natural medicine and medicinal chemistry, in particular to novel pentacyclic triterpene and melbine salt I of the derivative thereof. The salt compound can be used for preparing medicaments curing diabetes mellitus and complicating disease thereof, cerebral ischemia, angiocardiopathy, atherosclerosis, hepatitis, fatty liver and metabolic syndrome or tumour, descendens blood fat drugs and anti-obesity drugs. The invention also relates to the preparation method of the salt compound.
CN201701515U Artemisinine compound suppository for treatment of female genital disease The utility model discloses an artemisinine compound suppository for treatment of female genital diseases, which comprises a main suppository body. The main suppository body is provided with a through groove, and the through groove is of a nonconventional shape or a straight groove with a closed extending end. The through groove can comprise more than two communicated through grooves with any shape or can be the straight groove. With the through groove, the utility model realizes the easy pushing and pulling of such items as cotton swabs with the diameters smaller than the aperture of the through groove. When being needed, the artemisinine compound suppository is arranged in the vagina, and the cotton swab is inserted in the through groove, the artemisinine compound suppository is pushed by the cotton swab into the vagina, and then the cotton swab is pulled out of the through groove and the vagina. The utility model has the advantages of novel structure, safe and hygienic operation and convenient and rapid use, and can be easily absorbed by the human body.
US20110136748 Novel glucopyranose derivatives, preparation thereof, and biological uses thereof The invention relates to a novel ester, the 3,5-di-tertiobutyl-4-hydroxybenzoate of 3,4,5-trihydroxy-6-methoxytetrahydropyran-2-yl methyl defined by the following formula (I). The invention also relates to the method for preparing the compound of formula (I) and to the use of said compound (I) to prepare a drug for treating and/or preventing enveloped virus infections.
US20100256095 Compounds, methods and pharmaceutical compositions for inhibiting parp The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.
CA2105867C Novel imidazole derivatives, their preparation and therapeutic applications The present invention concerns new imidazole derivatives having the following general formula (IA) or (IB) (see formula IA or IB) which show useful binding property for histamine H3 receptors. The invention also concerns a process for the preparation of said compounds, and pharmaceutical compositions incorporating the same, in particular, useful as sedative, sleep regulating, anticonvulsant, psychostimulating, cerebral circulation modulating and anti-ulcer agents.
US7825129 Thieno[2,3-c] isoquinolines for use as inhibitors of PARP The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula: wherein the constituent variables are as defined herein. The invention further provides methods for the use of the compounds disclosed herein.
CN102440954A Thiamphenicol suspension emulsifier and preparation method thereof The invention relates to a thiamphenicol suspension emulsifier and a preparation method thereof. The thiamphenicol suspension emulsifier is prepared by the following components in weight percentage: 10-30% of micronized thiamphenicol, 5-15% of emulsifier, 20-30% of oil phase, 0.02-5% of auxiliary stabilizer and the rest of water, and has the advantages that the drug is a mixed system comprising a water phrase, the oil phrase and a solid phrase, the good characteristics of an suspension and an emulsifier are achieved, so that the intramuscular injection dosage is reduced, the stimulation in the body of a livestock is reduced, and after the drug is applied in the livestock, micronized drug active ingredients which are scattered in the water phrase and the oil phrase are slowly released in the body to realize the targeted, slow-release and long-acting functions. In addition, the preparation has large drug-loading quantity and stable quantity, is not easy to laminate and sediment after standing and transportation, and has good flowability so as to be injected in the body of the livestock. The thiamphenicol suspension emulsifier opens a new path for the application of thiamphenicol in veterinary clinic.
CN1906302B Genetically modified plants comprising SARS-CoV viral nucleotide sequences and methods of use thereof for immunization against SARS The invention relates to genetically modified plants and progeny thereof which constitute edible plant-derived mucosal vaccines and injectable plant-derived mucosal vaccines against Severe Acute Respiratory Syndrome (SARS). The invention relates to a recombinant vector that transforms specifically, but not limited to, the nuclei and/or plastids of tobacco, tomato and lettuce plants for antigen production. In specific embodiments, the plastid transformation vector expressing the nucleotide sequences are pCV1, pCV6 and pCV8, and their derivatives containing an S1 with nucleotide (but not amino acid) changes to optimize codon usage for expression in plants. The present invention relates to methods of making the modified plants which comprises transformation of plants with vectors for nuclearexpression and/or plastid expression of nucleotide sequences of the SARS-CoV virus, fragments, derivatives, analogs, or variants thereof. The present invention also relates to methods of immunizationagainst SARS and methods of antibody detection using the SARS-CoV antigens generated by the plastid and/or nuclear vector(s) transformed plants.
CN102397285A Application of hyperin in preparation of medicines for resisting vascular dementia The invention provides the application of a natural product such as hyperin in the preparation of medicines for resisting vascular dementia. By the verification of an in-vivo animal test, the hyperin can effectively restrain the histomorphology change of a vascular dementia rat, improve the acknowledgement, learning and memory ability of the vascular dementia rat and obviously relieve the symptom of the vascular dementia.
EP2523953A1 Preparation of 4-amino-thiazoles and 3-amino-1,2,4-thiadiazoles and their use as allosteric modulators of metabotropic glutamate receptors The present invention relates to novel compounds of Formula (I), wherein M, P, X, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors - subtype 4 ("mGluR4") which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
CN101313944B Herbal pain penetrating fluid The invention relates to a health care penetrant for external use, in particular to a health care penetrant auxiliarily used on a therapeutic device. The health care penetrant of the invention is prepared through taking the following materials in weight portion by the following steps: 40 to 60g of Wushe, 40 to 60g of centipede and 40 to 60g of scorpion are immersed in 2,500 to 5,000g of distilledspirit with a alcohol content more than 65 DEG for 10 to 20 days, and the liquor is taken; 20 to 40g of olibanum, 20 to 40g of myrrh, 20 to 40g of sting of gleditsia sinensis lam, 20 to 40g of monkshood root, 20 to 40g of kusnezoff monkshood, 30 to 50g of angelica, 30 to 50g of eucommia bark and 30 to 50g of safflower are boiled with water, and medicinal juice obtained is taken; 20 to 30g of clematis root, 30 to 50g of root of pseudo-ginseng, 30 to 60g of leech and 10 to 15g of borneol are immersed in 2,500 to 5,000g of 75 percent ethanol for 7 to 20 days, and the liquid after immersion is taken; and all three liquids are mixed evenly to prepare the penetrant of the invention. The penetrant has certain curative effects of treating diseases and symptoms such as shoulder pain, waist pain, leg pain, foot pain, hyperosteogeny, rheumatism arthralgia and injury of soft tissues, etc.
WO2008099883A1 Therapeutic agent for liver cancer Disclosed is a therapeutic agent for liver cancer or a cancer metastasis suppressor which comprising rifampicin or a derivative thereof as an active ingredient. An extensive study was made for the purpose of developing a therapeutic agent for liver cancer. As a consequence, it is found that rifampicin or a derivative thereof has a therapeutic effect on liver cancer, particularly metastatic liver cancer. Rifampicin or a derivative thereof has an activity of suppressing the proliferation of cancer metastasized to the liver and the invasion the cancer into a liver tissue, and has a therapeutic effect on metastatic liver cancer.
US7303758 From a two-layered polymeric matrix including incompatible polymers, the top layer controls elution rate of said drugs; e.g. fluoropolymer layer covered with a polyacrylate top layer; stents, anastomotic devices Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic drugs, agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the formation of blood clots. Also, the devices may be modified to promote endothelialization. Various materials and coating methodologies may be utilized to maintain the drugs, agents or compounds on the medical device until delivered and positioned. In addition, the devices utilized to deliver the implantable medical devices may be modified to reduce the potential for damaging the implantable medical device during deployment. Medical devices include stents, grafts, anastomotic devices, perivascular wraps, sutures and staples. In addition, various polymer combinations may be utilized to control the elution rates of the therapeutic drugs, agents and/or compounds from the implantable medical devices.
US20130053390 1-[(6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives The present invention relates to novel quinoxaline-piperazine compounds, 1-[(6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives and their pharmaceutically acceptable salts, a process for their preparation thereof, and compositions containing such compounds. Therapeutic methods for the treatment of hyperproliferative disorders, including cancers, by administering quinoxaline-piperazine compounds are also included.
US7022332 Sulfacetamide formulations for treatment of rosacea The present invention provides improved sulfacetamide and sulfur formulations including sunscreens for the treatment of rosacea.
US20100247628 Skin Treatment Compositions Containing Copper-Pigment Complexes This invention discloses compositions and method for treating various types of skin disorders, based on topical cutaneous delivery of copper chemically bound with botanical pigments. Sodium-copper-chlorophyllin is used as an example, showing benefits in the treatment of rosacea, acne, oily skin, enlarged pores, and in relieving skin inflammation. Benefits are also disclosed in treatment of environmentally caused premature skin aging, via reductions in fine facial lines and wrinkles, increased tensile strength of the skin, and increased protection against sunlight via increased production of melanin. Therapeutic outcomes are improved when the copper-pigment complex is enclosed within submicron liposomes.
WO2010011546A3 Pyrrolo [3, 2-b]pyridines and pyrazolo [4, 3 -b] pyridines having 5-ht6 receptor affinity The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, Q, G, Ar, m, and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
US7582778 Podophyllotoxin The invention relates to podophyllotoxins, uses thereof and methods of their production.
CN102973522A Application of salvianolic acid A lyophilized powder for preparing medicament for rescuing ischemic penumbra The invention relates to application of salvianolic acid A lyophilized powder in preparing a medicament for rescuing ischemic penumbra. The salvianolic acid A lyophilized powder comprises the following components by weight: 20 to 60g of salvianolic acid A, 20 to 60g of filler, and an antioxidant which accounts for 0.02 to 0.1 percent of the total preparation amount.
CN103463044A Application of Lycojaponicumin A in drugs for treating skin cancer The invention discloses application of Lycojaponicumin A in preparation of drugs for treating skin cancer and belongs to the technical field of new application of drugs. In vitro MTT anticancer activity evaluation discovers that Lycojaponicumin A shows remarkable inhibitory effects on growth of human skin cancer cell lines A431, HME1, A375 and SK23. Therefore, the Lycojaponicumin A can be used for preparing anti-skin cancer drugs, and has good development and application prospects. Application of the Lycojaponicumin A in preparation of drugs for treating skin cancer is disclosed for the first time; and because skeleton type is completely new, inhibitory activity on skin cancer cells is extraordinary strong.
WO2009005338A2 Solid forms ult-i, ult-2 and ult-3 of emtricitabine The present invention provides novel crystalline forms of Emtricitabine, designated Emtricitabine form ULT-I, form ULT-2 and ULT-3, methods for the preparation of Emtricitabine form ULT-I, ULT-2 and ULT-3 and the use of Emtricitabine form ULT-I and/or ULT-2 and/or ULT-3 in pharmaceutical applications, in particular in anti-HIV medicaments. The crystalline form of Emtricitabine form ULT-I, ULT-2 and/or ULT-3 can be used in combination with other anti-HIV medicaments such as Efavirenz and Tenofovir DF.
US7015214 Such as 7-chloro-2-cyanoimino-5-(cyclopropylmethyloxy)-1,5-dihydro-5-trifluoromethyl-1,3-benzodiazepine The present invention relates to 1,3-benzodiazepin-2-ones and 1,3-benzoxazepin-2-ones of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
WO2013163758A1 Methods for treating and diagnosing blinding eye diseases This invention relates to, in part, methods and compositions that are useful for the diagnosis, treatment, or prevention of a blinding eye disease, including in the discovery of drugs that are efficacious against these diseases. Diseases include, for example, age related macular degeneration and reticular pseudodrusen disease, and the methods described herein include, for example, the method named delayed near infrared analysis (DNIRA).
CN101352432B Technique of preparing nano vitamin E emulsion The invention relates to a technology for preparing nanometer vitamin E nano-calpis, which comprises the steps that under the condition of surface active agent, vitamin E is heated up and stirred to be made into stable o/W type calpis, and the dosage of the surface active agent is 15-25% of the vitamin E. The method has reliable method and causes no environmental pollution, and the obtained vitamin E nano-calpis is easier to be absorbed by the human body.
CN101347388A Oral cavity nursing agent and preparation technique thereof The invention provides a dental conditioning agent containing biologic activity hydroxyapatite or nano-hydroxyapatite and nano silver ion. The dental conditioning agent used for preventing and curing oral diseases comprises 5-10 weight percent of the biologic activity hydroxyapatite or the nano-hydroxyapatite and 1-5 weight percent of the nano silver ion. The effective repairing effect of the biologic activity hydroxyapatite or the nano-hydroxyapatite for the wound surface of the osseous tissue and the soft tissue of the human body and the strong sterilization function of the nano silver ion are used for preventing and curing a plurality of dental diseases, including decayed tooth, hemodia, tooth mobility, periodonititis, gingivitis, gingival atrophy, oral ulcer, halitosis and the pathologic change of oral mucosa, etc. And the dental conditioning agent can be made into various medicament forms, such as powdered drug, paste, teeth patch, cataplasm, aqueous solution, jellies and mouth wash, and the like, according to needs, thus facilitating the daily life use and the clinical use. In addition, the dental conditioning agent has the advantages of good curative effect, intensive medicament forms, easy manufacture, without drug tolerance, safety and no irritation.
WO2008058366A1 Oil-in-water emulsions, methods of use thereof, methods of preparation thereof and kits thereof An oil-in-water emulsion comprising at least one triglyceride oil, macrogol 15 hydroxystearate and a dispersing aqueous phase is described. Compositions, such as pharmaceutical compositions, and kits comprising the emulsion are also disclosed. Methods of preparing, as well as uses of, such emulsion and/or compositions are described. The emulsions and compositions of the invention are suitable for improving/increasing the stability, solubility and/or delivery of hydrophobic compounds.
WO2007143824A1 Azacyclopentane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase Azacyclopentane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.
US20100249235 Administration of 3,5-diiodothyropropionic acid for stimulating weight loss, and/or lowering triglyceride levels, and/or treatment of metabolic syndrome The invention provides methods and compositions for stimulating weight loss or lowering triglyceride levels in an individual in need thereof. In methods of the invention, a pharmaceutical composition comprising a therapeutically effective amount of DITPA, and optionally one or a plurality of lipid lowering agents, is administered to an individual to stimulate weight loss, lower triglyceride and/or lipoprotein levels, and/or to treat one or more symptoms of metabolic syndrome.
EP1968958A1 Substituted thiazoles and their use for producing drugs The invention relates to the substituted thiazoles of formula (I), to methods for producing them, to drugs containing said compounds and to the use thereof for producing drugs, preferably in drugs for treating pain.
US20100292331 Biomarkers for Prostate Cancer and Methods Using the Same Methods for identifying and evaluating suites of biochemical and/or gene entities useful as biomarkers for early prediction of prostate cancer, disease grading, target identification/validation, and monitoring of drug efficacy are provided. Also provided are suites of small molecule entities as biomarkers for prostate cancer.
WO2011032903A1 Piperazinyl-alkyl-benzoimidazol-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors The present application discloses novel piperazinyl-alkyl-benzoimidazol-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention discloses the use of these compounds in a method for therapy, and pharmaceutical compositions comprising the compounds of the invention.
EP1767201B1 Nutrient composition and composition for prevention/mitigation of digestive tract depression A nutrient composition which improves the depressed function of the digestive tract and is effective in preventing/mitigating the diarrhea, regurgitation in the stomach/esophagus, and erroneous swallow which accompany the administration of a liquid nutrient; and a composition for the prevention/mitigation of digestive tract depression. The nutrient composition and the composition for the prevention/mitigation of digestive tract depression are characterized by containing at least one member selected among glutamic acid, 5'-nucleotides, and salts of these, and further characterized in that when glutamic acid only is contained therein, thecontent thereof is 0.0013-1.3 w/v% in terms of free glutamic acid amount at the time of administration.
EP1263746B1 Substituted 8, 8a-dihydro-3ah-indeno 1,2-d]thiazoles, a method for their production and their use as medicaments The invention relates to substituted 8, 8a-dihydro-3aH-indeno[1,2-d]thiazoles and to their physiologically compatible salts and physiologically functional derivatives. The invention relates to compounds of formula (I), wherein the groups have the given meanings, to their physiologically compatible salts and to a method for their production. The compounds are, for example, suitable for use as anorectic agents.
US20090018104 Triarylcarboxylic Acid Derivative Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.
EP2043654A2 Thienopyrimidines useful as modulators of ion channels The present invention relates to compounds of formula (I) useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
US20100305060 Nucleoside Prodrugs and Uses Thereof This application provides compositions or compounds as disclosed herein that are suitable for treating hepatic viral diseases, such as hepatitis C(HCV).
US20090312313 Compound having tgfbeta inhibitory activity and pharmaceutical composition comprising the same The present invention provides compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein X represents CH or N; Z represents —O—, —NH— or —C(═O)—; R and R′ represent a hydrogen atom, hydroxyl, a halogen atom, optionally substituted alkyl, optionally substituted alkenyl optionally substituted alkoxy, amino, aminocarbonyl, or an optionally substituted heterocyclic group; and A represents an optionally substituted specific carbocyclic or heterocyclic group. The compounds according to the present invention have excellent TGFβ inhibitory activity.
US20090226511 Novel pharmaceutical formulation in the form of cellulose capsules suitable for benzimidazole derivatives A filled cellulose capsule for oral administration, wherein the capsule comprises a cellulose derivative as the base and the filling comprises a therapeutically effective amount of a benzimidazole derivative but does not comprise a lower-substituted hydroxypropyl cellulose (13 to 16% hydroxypropoxy groups) is disclosed.
US20100130524 Therapeutic or prophylactic agent for dyskinesia An object of the present invention is to provide a drug with a high therapeutic or prophylactic effect on dyskinesia, without accompanying aggravation of symptoms of the primary disease, and with fewer side effects. Accordingly, the present invention provides a therapeutic or prophylactic agent for dyskinesia, comprising as an effective component a compound having a 4,5-epoxy morphinan skeleton, which compound is represented by the Formula (I) below, or a pharmaceutically acceptable acid addition salt thereof: [wherein the double line composed of a dashed line and a solid line represents a double bond or single bond, R1 is C4-C7 cycloalkylalkyl, R2 is C1-C5 straight or branched alkyl, and B is —CH═CH—.]
US8546334 Device having osteoinductive and osteoconductive properties The present invention relates to a device having osteoinductive and osteoconductive properties in vivo comprising a carrier containing calcium phosphate and an osteoinductive protein, wherein the carrier is homogenously coated with the protein. Moreover, the present invention relates to a method for the production of a device having osteoinductive and osteoconductive properties in vivo. The invention encompasses a pharmaceutical composition comprising the device of the invention or a device which is obtainable by the method of the invention and relates to the use of the device for the preparation of a pharmaceutical composition to be used for bone augmentation, for treating bone defects, for treating degenerative and traumatic disc disease, for treating bone dehiscence or to be used for sinus floor elevation. Finally, the invention relates to a kit comprising the device of the invention or a device which is obtainable by the method of the invention.
WO2007045593A2 Naphthyl derivatives as inhibitors of beta-amyloid aggregation Compounds useful in the treatment of disorders characterised by deposits of amyloid aggregates are herein described together with pharmaceutical compounds containing the same. In particular the compounds of the present invention are those having the Formula (I) as reported below. where the radicals have the meaning indicated in the description.
US20120184608 N alkylcarbonyl amino lactone compounds and their use The present invention generally relates to refreshing, soothing, and cooling compounds that affect sensory processes. More particularly, the present invention pertains to certain N-alkylcarbonyl-amino lactone compounds as described herein; compositions and articles comprising such compounds; and methods of treatment, for example, methods of alleviating the discomforts of irritation, itch, and pain in the skin and in the linings of the oral cavity and upper respiratory tract, for example, in methods of treatment of cough.
WO2011079076A1 Substituted n-(1h-indazol-4-yl)imidazo[1, 2-a]pyridine-3- carboxamide compounds as cfms inhibitors Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4 and R5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.
US20120009248 Preservation of Bioactive Materials By Spray Drying This invention provides methods and compositions to preserve bioactive materials in a matrix of powder particles. Methods provide high-pressure gas spraying and/or near supercritical spraying of formulations followed by drying in a stream of conditioned gas to form stable powder particles containing bioactive materials.
WO2010019953A1 High concentration local anesthetic formulations for treating non-neuropathic pain A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours.
WO2012168665A1 Novel agomelatine cocrystals, method for preparing same, and pharmaceutical compositions containing same The invention relates to an agomelatine cocrystal consisting of: the agomelatine or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide of formula (I); and a solid organic acid.
CN103755659A 6-cinnamon acyl-2H-benzo [b] [1, 4] oxazine-3 (4H)-ketone compound and application thereof The invention discloses a 6-cinnamon acyl-2H-benzo [b] [1, 4] oxazine-3 (4H)-ketone derivative and application thereof, wherein a structural general formula of the derivative is shown in Formula (I), and Ar in the formula represents an aryl. Pharmacological experiments show that the compound provided by the invention has an obviously inhibiting effect on the proliferation of lung carcinoma cells A549, and indicate that a chalcone derivative containing benzoxazine ketone disclosed by the invention has development prospects in clinical applications and has important values in the exploitation of anti-tumor drugs.
US20120020923 Method of treating viral diseases with combinations of TPO receptor agonist and anti-viral agents Invented is a method of treating viral diseases, particularly hepatitis C, in a human, in need thereof which comprises the administration of a combination of therapeutically active agents selected from a TPO receptor agonist and an antiviral therapy selected from: an alpha interferon, ribavirin, a ribavirin analog and an HCV antiviral to such human.
EP1832291A2 use of pyridoxal phosphate for the treatment of diabetes and related complications Use of pyridoxal-5'-phosphate, a pharmaceutically acceptable acid addition salt thereof, or a mixture thereof for the preparation of a medicament for treating insulin-dependent or non-insulin-dependent diabetes mellitus, related conditions, symptoms of insulin-dependent or non-insulin-dependent diabetes mellitus, or related conditions, or any combination thereof in a mammal.
WO2011121151A1 Functional food supplement intended, in particular, for nutrition and for prevention and improvement in cases of neurological alterations, neurodegenerative alterations or cognitive disorders The invention relates to a functional food supplement intended to supplement nutrition by enteral or oral delivery in the case of patients with neurological or neurodegenerative alterations, as well as to prevent states of cognitive or behavioural deterioration, particularly in the elderly. The functional ingredient, which has been specially formulated for the nutrition of patients suffering from or likely to develop neurological or neurodegenerative alterations, cognitive deterioration or behavioural disorders, comprises a mixture of UMP (uridine monophosphate or uridine) and/or IMP (inosine monophosphate or inosine), B group vitamins (B1, B6, B9 and B7), phospholipids and gangliosides, sialic acid, as well as a high proportion of DHA.
US20110065778 RNA Interference Mediated Inhibition of Muscarinic Colinergic Receptor Gene Expression Using Short Interfering Nucleic Acid (siNA) The present invention relates to compounds, compositions, and methods useful for modulating the expression of genes associated with respiratory and pulmonary disease, such as cholinergic muscarinic receptor genes, using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of cholinergic muscarinic receptor genes, or other genes involved in pathways of cholinergic muscarinic receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of M3 muscarinic acetylcholine receptor or cholinergic receptor muscarinic 3 (CHRM3).
WO2007147478A1 3 -amino-imidazo[1, 2-a]pyridine derivatives as sglt inhibitors Disclosed are novel compounds of formula (I), wherein X, Y, R, R', R1, R1', R1', R2, R2', R2', R3, R3', R4, R4', and n have the meanings indicated in claim 1. Said novel compounds are suitable as antidiabetics.
CN101088563A Anticancer composition containing lomustine The anticancer composition includes effective anticancer component selected from tyrosine kinase inhibitor and/or lomustine and slow releasing supplementary material, and may be prepared into slow released injection and slow released implant. The slow released injection includes also suspending agent and special solvent. The suspending agent has viscosity at 20-30 deg.c of 100-3000 cp and is selected from sodium carboxymethyl cellulose, etc. The slow releasing supplementary material is selected from p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP/TC), p(BHET-EOP/TC), p(BHDPT-EOP/TC), p(BHDPT-EOP/TC), p(CHDM-HOP), p(CHDM-EOP), etc. The released injection and slow released implant may be injected or set in tumor for slow releasing to maintain high medicine concentration for over 60 days to raise the treating effect and lower the systemic reaction on the medicine.
WO2012034189A1 Methods of using mirnas transcribed from the 14q32 region of human chromosome 14 as biomarkers for schizophrenia or symptoms thereof Provided herein are methods for detecting a risk profile for schizophrenia or a manifestation thereof or a sub-threshold phenotype or state thereof in a subject, comprising identifying a reduction or down regulation in expression of one or more miRNAs disclosed herein, or a molecule that regulates the expression of said miRNA, in blood from the subject wherein the reduction or down regulation of expression is indicative of a risk of the subject having or developing symptoms of schizophrenia. Also provided are methods of diagnosing schizophrenia based on the expression profiles of the miRNAs and miRNA regulatory molecules disclosed herein, and methods for treating schizophrenia by modulating the expression of said miRNAs and regulatory molecules.
CN1593402A Application of di-amino di-indoly cyclo-nonanoyl imide in the process for preparing anti-tumor medicine The invention relates to the use of diamino bisindole nonanoyl imide, in particular the use in preparing antineoplastic medicaments, therein the prepared medicament is safe and non-toxic, and has substantial immunity facilitation function.
US20050256134 Use of creatine analogues and creatine kinase modulators for the prevention and treatment of glucose metabolic disorders The present invention relates to the use of creatine compounds including cyclocreatine and creatine phosphate for treating or preventing a metabolic disorder consisting of hyperglycemia, insulin dependent diabetes mellitus, impaired glucose tolerance, hyperinsulinemia, insulin insensitivity, diabetes related diseases in a patient experiencing said disorder. The creatine compounds which can be used in the present method include (1) analogues of creatine which can act as substrates or substrate analogues for the enzyme creatine kinase; (2) compounds which can act as activators or inhibitors of creatine kinase; (3) compounds which can modulate the creatine transporter (4) N-phosphocreatine analogues bearing transferable or non-transferable moieties which mimic the N-phosphoryl group. (5) compounds which modify the association of creatine kinase with other cellular components.
EP2611448A1 7-cyclylquinazoline derivatives and methods of use thereof Provided herein are 7-cyclylquinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase- mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
CN103041137A Pharmaceutical composition for preventing and treating senile dementia, and preparation method thereof The invention relates to a pharmaceutical composition for preventing and treating senile dementia, and a preparation method thereof. The pharmaceutical composition has the effects of delaying senescence, nourishing liver and kidney as well as replenishing the vital essence and promoting mentality.
CN102000018B Solid dispersion containing celecoxib as well as preparation method and application thereof The invention relates to a solid dispersion containing celecoxib as well as a preparation method and application thereof. The invention needs to solve the technical problems of difficult pulverization of raw materials and difficult preparation of solid oral preparation of celecoxib. The solid dispersion is a solid dispersion containing the celecoxib and polyethylene glycol which are in the weightratio of 1:0.5-10. The preparation method comprises the following steps of: melting solid polyethylene glycol by heating, adding the celecoxib and dissolving to obtain a clear solution; or mixing andheating the solid polyethylene glycol and the celecoxib, and melting to obtain a clear solution; and then rapidly cooling to obtain the solid dispersion. The solid dispersion can be prepared into various oral preparations after being pulverized.
CA2359027C S-nitrosothiols as agents for the treatment of circulatory dysfunctions Novel S-nitrosothiols derivatives of penicillamine or glutathione, which correspond to following general formula(I) (see formula I) in which: A and B are phenyl groups or together form the rest -CH2-Q-CH2- constituting a ring of six units in which Q represents an atom of oxygen, of sulfur, or a group N-R3, in which R3 is hydrogen or an alkyl group C1-C4; R1 is an acyl rest, which may be an aliphatic acyl group C1-C5 or a rest of glutamic acid bound via its non amino acid carboxyl; R2 is a hydroxyl group or a glycine rest bound via a peptide bond;with the proviso that if R1 is an aliphatic acyl rest then R2 is a hydroxyl group, and if R1 is a rest of glu-tamic acid then R2 is a glycine rest. The novel compounds have vasodilating activity arid inhibit the aggregation of the platelets, which make them useful for the treatment of dysfunctions of the cir-culatory system, specially at cardiovascular level.
CA2559552A1 Benzyl-pyridazinone derivatives as non-nucleoside reverse transcriptase inhibitors The present invention relates to a compounds according to formula (I), methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula (I) and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula (I) where R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
CN101259129A Combined treatment for acute leukemia and myelodysplastisches syndrom The invention provides a therapeutic method of acute leukaemia such as acute medullary leukaemia and myeloproliferative disorder syndrom and a medicinal composition thereof. Anti-CD33 cytotoxic conjugate and at least one compound selected from anthracycline and pyrimidine or purine nucleoside analogs are adopted by the therapeutic method and the medicinal composition Gemtuzumab ozogamicin, daunomycin and cytosine arabinoside are adopted in a preferential therapeutic method and medicinal composition.
CN102584615A Alkaloid compound as well as preparation method and application thereof The invention discloses an alkaloid compound as well as a preparation method and an application of the alkaloid compound. The alkaloid compound has a molecular formula of C15H21NO4. The preparation method of the alkaloid compound comprises the steps that activated Pestalotiopsis sp. fungi Z233 are inoculated into culture liquid, and the fermentation culture is carried out for 10 to 40 days at 20 to 30 DEG C; mycelia and fermentation liquid are obtained through separation after the fermentation culture; after the mycelia are leached, extracted and concentrated by organic solvents, mycelium extractives are obtained; or the fermentation liquid is extracted and concentrated to obtain fermentation liquid extractives; and the chromatographic separation and the purification treatment are carried out on the mycelium extractives or the fermentation liquid extractives, and the alkaloid compound is prepared. The alkaloid compound with a novel structure is extracted and separated from fermentation culture substances of Sargassum horneri epiphytic Pestalotiopsis sp. fungi Z233, and the alkaloid compound has better antitumor activity, can be used for preparing antitumor medicine and tumor prevention health-care food and has good development prospects.
CN101671382B Ultra-micronized megestrol acetate and pharmaceutical composition containing same The invention relates to an ultra-micronized megestrol acetate in which 100% of particle sizes are smaller than or equal to 10 mu m. The invention also relates to a pharmaceutical composition containing the ultra-micronized megestrol acetate, which comprises an effective quantity of ultra-micronized megestrol acetate and medically acceptable excipient, wherein the effective quantity is 80-160 mg of ultra-micronized megestrol acetate. The pharmaceutical composition can be prepared into dispersing tablets, common tablets and capsules and used for treating advanced breast cancer, advanced endometrial carcinoma, renal carcinoma, prostatic cancer and oophoroma, and can improve the appetite and the cachexia of patients with advanced tumors.
CN102698171A Dedicated drug for treatment of breast cancer A dedicated formula of the invention for treatment of breast cancers comprises: glycyrrhiza uralensis fisch, black seed of soybean, bulbus fritillaria, rhizoma cimicifugae, resina populi, ciliatenerve knotweed with leaves and stems, musk, patrinia scaniosaefolia, pedicularis verticillata, swork jackbean seed, er cao, flos caryophyllata, bottle gourd leaves, pinus tabulaeformis Carr., shebeipa, fluorite, hygrophila salicifolia (vah) nees roots, barbated skullcup herb, a processed dry duck leg, a processed dry goose leg, a processed dry pigeon leg, a processed dry chicken leg, and a processed dry Chinese marine large prawn leg. A preparation method includes the steps of: grinding to fine powder, and making sheets for oral administration.
US20090238859 Sinus delivery of sustained release therapeutics The invention provides biodegradable implants for treating sinusitis. The biodegradable implants have a size, shape, density, viscosity, and/or mucoadhesiveness that prevents them from being substantially cleared by the mucociliary lining of the sinuses during the intended treatment period. The biodegradable implants include a sustained release therapeutic, e.g., an antibiotic, a steroidal anti-inflammatory agent, or both. The biodegradable implants may take various forms, such as rods, pellets, beads, strips, or microparticles, and may be delivered into a sinus in various pharmaceutically acceptable carriers.
CN102106901A Liniment for treating skin diseases of dogs and cats, and preparation process thereof The invention discloses a liniment for treating skin diseases of dogs and cats, and a preparation process thereof. The liniment is composed of lightyellow sophora root, Chinese mugwort leaf, bothriospermum chinense, menthol crystal, camphor and a nitro imidazole medicament; and the method for preparing the liniment comprises the following steps: extracting the lightyellow sophora root, the Chinese mugwort leaf and the bothriospermum chinense, or directly utilizing the extracts thereof; then sequentially adding the menthol crystal, the camphor and the nitro imidazole medicament to the extracts; and uniformly mixing.
US20110002851 Cationic Colloidal Carriers for Delivery of Active Agents to the Blood-Brain Barrier in the Course of Neuroinflammatory Diseases The present invention relates to the use of cationic colloidal compositions for the targeted delivery of an active compound to an inflammatory site or an activated vascular site for the preparation of a medicament for the treatment of MS and in general for all CNS or PNS inflammatory neurodegenerative and demyelinating diseases and for diagnostic applications of such compositions.
CN101044136A Pyrrolo-naphthyl acids as pai-1 inhibitors The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
EP1518858A1 Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments The invention relates to the polymorph A of flibanserin (1), to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.
US20070299103 [1,2,4]Triazolo[4,3-A]Pyridine Derivatives for the Treatment of Hyperproliferative Diseases The invention provides novel, substituted 7-arylamino[1,2,4]triazolo[4,3-a]pyridine compounds Formula (I): pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10 R11, R12, R13, R14 and L are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
CN103083248A Polysaccharide sulfate dry suspension The application relates to dry suspension, and particularly relates to polysaccharide sulfate dry suspension.
CN102659746A Ailanthus flower extract as well as preparation method and application of active ingredients brevifolin of ailanthus flower extract The invention provides an ailanthus flower extract as well as a preparation method and an application of active ingredients brevifolin of the ailanthus flower extract. The ailanthus flower extract and a total isocoumarin active part are prepared through researching the chemical components of ailanthus flower, and three types of cyclopentanone isocoumarin, i.e. brevifolin, brevifolin-carboxylic acid and methyl brevifolincarboxylat are obtained through separation. A biological activity research shows that the ailanthus flower extract has the remarkable anti-oxidation, anti-inflammation and anti-tumor effects. Experimental results show that the ailanthus flower extract (including effective part) and ailanthus flower elements with active compounds can be used for preparing drugs and health care products for oxidation resistance, inflammation resistance, tumor resistance and other relevant diseases treatment.
CN102920779A Externally-applied preparation having blood circulation promoting, blood stasis removing, meridian dredging and vein relaxing functions, and its preparation method An externally-applied preparation having blood circulation promoting, blood stasis removing, meridian dredging and vein relaxing functions comprises the following components, by weight, 30-60 parts of Cassia Twig, 20-40 parts of Herba Taraxaci, 30-60 parts of Radix Angelicae Pubescentis, 30-60 parts of Chinese angelica, 10-20 parts of Manchurian wildginger, 60-100 parts of Radix Aucklandiae, 30-60 parts of borneol and 30-60 parts of menthol. The preparation method of the externally-applied preparation comprises the following steps: extracting and purifying plant essential oil through a supercritical extraction device to collect volatile oil; adding water to drug residues obtained after the extraction of the volatile oil, refluxing, allowing the obtained filtrate to stand, centrifuging the drug filtrate through a high speed centrifugal machine, and filtering the centrifuged drug filtrate with a ceramic film to obtain a clear liquid; and co-dissolving the volatile oil and corresponding weights of the borneol and the menthol in glycerin, adding polyethylene glycol 400, adding a water extract which is the clear liquid, uniformly stirring, and filtering. The externally-applied preparation has the advantages of simple preparation method and substantial curative effects.
US6949539 Antiinflammatory agents; autoimmune disease; rheumatic disorders The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
US7255853 for topical use for protecting the skin and the hair Cosmetic compositions for topical use for protecting the skin and the hair, containing, in a cosmetically acceptable support, at least one compound of formula (1) or (2) in which X1 represents R3—(C═O)—, R3—SO2— or R3—O—(C═O)—, X2 represents —(C═O)—R′3—(C═O), —SO2—R′3—SO2— or —(C═O)—O—R′3—O—(C═O)—, Y represents —(C═O)—R4 or —SO2R5, R2 represents a C1-8 alkyl group, n is 0, 1 or 2, R3 represents C1-30 alkyl or C3-30 alkenyl, R′3 represents a single bond or a divalent C1-30 alkylene or C3-30 alkenylene radical, R4 represents —OR6 or —NHR6, R5 represents C1-30 alkyl or a phenyl nucleus, R6 represents C1-30 alkyl or C3-30 alkenyl, and novel compounds of formula (2).
CN1965818A Prescription for preparing high-quality tranexamic acid injection and preparation process thereof The invention relates to amino acid injection formula and relative agent, wherein said formula comprises 500g acidum transamicum, 0.5-25g stabilizer, 0.5-10g buffer, and 5000ml injection water; or 1000g acidum transamicum, 1.0-50g stabilizer, 1.0-20g buffer, and 10000ml injection water. And the production comprises that: weighting acidum transamicum, dissolving it into 80% injection water, adding stabilizer and buffer, adding water, adding injection active carbon, heating, mixing, filtering, checking, bottling, sealing and disinfecting. In the production, the Z-isomer has low content, and the amino acid has strong anticoagulant effect than 6-aminoacetic acid and PAMBA, but same hemostatic effect as aprotinin, with 1/60 cost.
CN103127079A Application of Aphanamixoid A in medicines curing stomach cancer The invention discloses application of Aphanamixoid A in medicines curing stomach cancer and belongs to the medicines new use technical field. An external MTT antineoplastic activity evaluation shows that the Aphanamixoid A has evident inhibiting effect on growth of human stomach cancer cell strain HGC-27, MGC-803, BGC-823 and SGC-7901. Therefore, the Aphanamixoid A can be used for preparing stomach cancer resisting medicines, and has good development and application prospect. Due to the fact that use of the Aphanamixoid A in preparation of the medicines curing the stomach cancer is made public for the first time, and the Aphanamixoid A has an unexpectedly high stomach cancer inhibitory activity.
CN102079739B Daidzein derivative, preparation method and application thereof The invention discloses a daidzein derivative, a preparation method and application thereof, relating to the daidzein and providing a daidzein derivative which is shaped as yellow gel and has a chemical name of 3',8-diallyl-4',7-dyhydroxyl isoflavone and the molecular weight of 334.1. The daidzein derivative can be conveniently and rapidly prepared through a Claisen rearrangement reaction, the preparation method is simple, and the used raw materials are low in price, thus the daidzein derivative can be widely applied to the industrial production. The 3',8-diallyl-4',7-dyhydroxyl isoflavone has a similar structural characteristics to the daidzein, but has remarkably improved antitumor activity compared with the daidzein. The daidzein derivative can remarkably inhibit the growth of tumor cells and can be widely applied to the preparation of the antitumor drugs.
WO2006033568A1 Synergistic composition for the treatment of diabetes and the comorbidites thereof The invention relates to the pharmaceutical industry in general and to the industry involved in the manufacture of pharmaceutical products for the treatment of diabetes and the comorbidites thereof. The invention is advantageous over prior art compositions in that it enables long-term management of diabetic symptoms in order to maintain adequate glycaemic control, such as to produce a more powerful effect in relation to hyperglycaemia, thereby enabling a reduction in doses and, consequently, the individual collateral effects of the drugs utilised. In addition, the inventive composition improves insulin sensitivity of pancreatic beta receptors, simultaneously correcting insulin secretion disorders, and stimulates lipid metabolism, thereby improving the profile of same in the blood plasma. The composition is formed by a hypoglycaemic agent, glimepiride, and an anti-hypoglycaemic agent, pioglitazone. The composition contains between 5 and 2,500 mg pioglitazone and between 1 and 250 mg glimepiride.
WO2007060540A1 Stable dosage forms of an antidepressant The present invention relates to stable solid dosage forms of an antidepressant. More particularly, the present invention relates to stable solid dosage forms of bupropion hydrochloride. The present invention also relates to a process for the preparation of stable solid dosage forms of bupropion hydrochloride.
US20060058392 Use of a rhein in a therapeutic treatment requiring a rise in the rate of heme oxygenase The invention concerns a novel therapeutic application of rhein and diacerhein. Rhein and diacerhein, as well as the salts and esters thereof, can be used for treating diseases requiring a rise in the rate of the heme oxygenase enzyme, providing prevention and inhibition of stress on cells and tissues, and treatment and prevention of organ and tissue transplant rejections.
CN101181357B Detection method of chlorphenamine Maleate of ketelin lozenge The invention relates to a quality control method of chlorpheniramine maleate of Keteling troche, which is characterized in that the method includes a chlorpheniramine maleate thin layer chromatographic method examination of the Keteling troche pressing grain, a content measurement of the chlorpheniramine maleate with high-efficiency liquid phase chromatography, a chlorpheniramine maleate thin layer chromatographic method examination of Keteling troche finished product and a content measurement of the chlorpheniramine maleate with high-efficiency liquid phase chromatography. The quality control method of the Keteling troche provided by the invention adopts the chromatography and the color developing conditions to lead the chlorpheniramine maleate to effectively separate from other ingredients, the test result has good repeatability; the content of the chlorpheniramine maleate can be precisely measured in the Keteling troche, and the quality of the Keteling troche finished product is effectively controlled.
CN101700252A Skin-care cream for treating skin cracks The invention relates to a skin-care cream for treating skin cracks, which is prepared from the following raw materials in parts by weight: 11-13 parts of vaseline, 0.028-0.032 part of vitamin E, 2.8-3.6 parts of honey, 0.001-0.003 part of anisodamine, 2.2-3.2 parts of glycerol and 1.8-2.6 parts of paraffin oil. The preparation method comprises the following steps: heating to dissolve the vaseline; decreasing the temperature of the vaseline to 45+/- 5 DEG C, adding the honey, and evenly mixing; adding the glycerol, and evenly mixing; gradually adding the paraffin oil, and evenly mixing; adding the vitamin E and the anisodamine, and evenly mixing into the cream; and packaging the cream into boxes. The skin-care cream can be widely used for treating cracks all over the body to achieve the effects of relieving pain, removing inflammation and healing wounds, and has the functions of antiphlogosis and antianaphylaxis for leg cracks, pruritus and desquamation in winter and spring. The skin-care cream has the advantages of quick curative effect, short curative period, favorable curative effect, high safety and no toxic or side effect, and can be taken orally, thereby being an ideal product for medical treatment, facial beautification, wrinkle resistance and skin care.
CN101250180A Amorphous S-pantoprazole sodium, preparation method and use thereof The invention relates to amorphous S-pantoprazole sodium, a relative preparation method and an application. The preparation method comprises (a) mixing S-pantoprazole and C1-3 alkyl alcohol, adding alkali compound with metal sodium ions and reacting, wherein the C1-3 alkyl alcohol is one of methanol, ethanol, propanol and isopropanol, whose added volume is 2-50 times of the mass of S-pantoprazole, and the alkali compound with metal sodium ion is one of sodium methanol, sodium ethanol, sodium propanol and sodium isopropanol, and the mol ratio between the alkali compound with metal sodium ions and the S-pantoprazole is 1:1, (b) adding ether into the reaction liquor to crystallize S-pantoprazole sodium, wherein the added amount of ether is 1-10 times of the volume of C1-3 alkyl alcohol, (c) filtering the crystallization liquid and drying in vacuum to obtain amorphous S-pantoprazole sodium, wherein the drying temperature is 20-50DEG C.
US20110311634 Formulations for animal feed comprising butyrate salt The present invention relates to formulations for animal feed comprising coated granules comprising butyrate salt; the butyrate salt is preferably the salt of sodium or calcium salt. The coated granules have a particle size of 0.1 mm or more, preferably 0.2 mm or more and about 2 mm or less, and preferably about 1 mm or less. The coated granules comprise a binder and a coating. Further, the butyrate salt can be combined with another active ingredient which may be chosen from the group consisting of plant extracts, prebiotic compounds, probiotics, yeast extracts, middle-length chain fatty acids, unsaturated long chain fatty acids, lactate salt, fat soluble vitamin, and toxin absorbing compound.
WO2006080430A1 Ophthalmic medicine composition An ophthalmic medicine composition, in particular, eye-drops, eye ointment, eyewash agent, intraocular perfusate, anterior chamber washing agent, internal medicine, injectable solution or extracted cornea preserving agent that excels in therapeutic efficacy and/or preventive efficacy for lens and/or cornea swelling, edema or clouding attributed to cataract and other ophthalmic diseases, and that is safe, permitting long-term continued administration. There is provided an ophthalmic medicine composition comprising a sugar having a fundamental cyclic structure composed of four glucose molecules bound together in circular form through specified binding mode and/or a derivative of the sugar.
US20100063018 orphan nuclear receptor modulators such as 23-N-Carbacinnamyloxy-3 alpha ,7 alpha -dihydroxy-5 beta -norcholanylamine, used for the treatment of liver, gastrointestinal, kidney, cardiovascular or metabolic disorders The present invention relates to compounds of formula (I) wherein: R1 is hydrogen or an alkyl group; R2 is hydrogen or a halogen, nitro, alkyloxy, amino or carboxy group; Y is CH2, oxygen or sulfur; n is an integer from 1 to 4, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof for the treatment of FXR-mediated diseases or conditions.
WO2010033977A2 Multiheteroaryl compounds as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).
EP2377875A1 Antioxidant To provide an antioxidant which is highly safe, inhibits oxidation of a biological component, in particular, a lipid, and is used as a drug, food or drink, a food additive, an external preparation for skin, or the like. The antioxidant contains 3-O-β-D-glucopyranosyl-4-methylergost-7-en-3-ol as an active ingredient.
US20080033052 Dermal anesthetic compounds The present invention relates to new tetralin compounds, the methods of preparing said tetralin compounds, the method of using said tetralin compounds as local anesthetics and dermal anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.
EP1268502B1 O-aryl glucoside sglt2 inhibitors and method Formula (I) wherein Y is formula (a) or heteroaryl; A is -O(CH2)m, S, -NH(CH2)m, or (CH2)n where n is 0-3 and m is 0-2; and R1 to R6 are as defined herein. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with one, two or more other antidiabetic agents, and/or one, two or more hypolipidemic agents.
US7220752 Liver selective glucocorticoid receptor antagonists; lowering blood glucose levels; 3,5-dibromo-4-(5-isopropyl-2-(3-methylbenzoyl)-4-(3-methyl-3-b utenyloxy)phenoxy)-phenylacetic acid for example This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein the variables are as defined herein.
US6872711 β-substituted β-aminoethyl phosphonate derivatives The present invention relates to novel β-substituted-β-aminoethylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.
CN103463116A Application of 20(S)-ginsenoside Rh2 in preparation of drugs enhancing antibacterial action of 4-quinolones The invention relates to application of 20(S)-ginsenoside Rh2 in preparation of drugs enhancing antibacterial action of 4-quinolones. The invention discloses that 20(S)-ginsenoside Rh2 can improve the therapeutic effect of ciprofloxacin on a mouse abdominal infection model, and can reduce the minimal inhibitory concentration (MIC) of ciprofloxacin in staphylococcus aureus ATCC 29213, 4 staphylococcus aureus clinical strains, and pseudomonas aeruginosa ATCC 27853. On a staphylococcus aureus invaded THP-1 macrophage model, 20(S)-ginsenoside Rh2 can enhance the intracellular antibacterial action of levofloxacin. Therefore, 20(S)-ginsenoside Rh2 is expected to be used for preparing a synergist of quinolone antibiotics, and can be developed into assistant drugs of anti-infective therapy.
US8604021 Substituted arylamine compounds and methods of treatment The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.
US20080184618 Adsorbing, binding deactivated viruses; therap for mammals infections; gastrointestinal disorders Layered phyllosilicates are useful for adsorbing and/or binding to and, thereby, inactivating viruses. Accordingly, provided herein are methods of inactivating a virus and methods of treating a viral infection. Methods of delivering a therapeutic agent to a mammalian subject and methods of inactivating a virus in the gastrointestinal tract of an animal are also provided.
US20110002992 N-sulphonylated amino acid derivatives, method for the production and use thereof The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.
EP1429757B1 Crystalline forms of fluvastatin sodium Novel crystalline forms of Fluvastatin sodium hydrates were found, referred to hereinafter as polymorphic Forms C, D, E and F. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms, a process for the preparation of highly crystalline Fluvastatin sodium Form A, and pharmaceutical compositions comprising the crystalline forms.
US20090143280 Anti-cancer combination treatment and kit-of-parts In one aspect the present invention relates to pharmaceutical kits of parts suitable for treating neoplastic diseases such as cancer comprising an anti-cancer medicament, a Basidiomycete bioactive agent in solid or liquid form, and, optionally instructions for a dosing regime.
CN102552212A Soft capsule for improving cranial nerve function and preparation method thereof The invention relates to a soft capsule for improving the cranial nerve function and a preparation method thereof. The soft capsule comprises content and a capsule shell material; the content comprises glyceryl phosphoryl choline and a solvent, wherein the glyceryl phosphoryl choline accounts for 60-95% of the total weight of the content; the solvent accounts for 5-40% of the total weight of the content; the solvent comprises one or several of water, glycerol, sorbitol, sorbitan, glycerol triacetate, polyethylene glycol 200, polyethylene glycol 400 and propylene glycol; and the capsule shell material comprises one or several of gelatin, water, glycerol, sorbitol, sorbitan, methylparaben, ethylparaben, propylparaben, titanium dioxide and iron oxide yellow. The preparation method comprises the following steps of: pressing a solution A prepared by the glyceryl phosphoryl choline and the solvent and a solution B prepared by the capsule shell material into soft capsules by a soft capsule machine; and drying to obtain the soft capsule for improving the cranial nerve function.
CN1951359A Multi-element compound physical therapeutic salt and preparation method thereof The invention relates to a multifunctional composite physiotherapy salt, which at least comprises common salt (NaCl), mirabilite (Na2SO4) and/or potassium chloride (KCl), calcium sulfate (CaSO4), calcium hydrogen orthophosphate (CaHPO4), addex-magnesium (MgSO4 ) and/or bichloride cobalt (CoCl2*aH2O), zinc sulfate (ZnSO4) and copperas (FeSO4). The invention also provides relative production. The invention can loose the hair, diminish the inflammation and reduce the pain, etc.
EP2220032A1 Novel solvate The present invention relates to the novel crystalline form X of Tigecycline and to processes of preparing the same. Furthermore the present invention relates to the use of crystalline form X of Tigecycline as an intermediate for the preparation of an anti-infective medicament. Moreover the present invention relates to the use of crystalline form X of Tigecycline for the preparation of acid addition salts of Tigecycline
US20060252839 Cyclopenteneones for antiischemic agents, antiinflammatory agents and aging resistance A compound comprising a cyclopentanone, cyclopentenone, cyclohexanone or cyclohexenone group, wherein a first ring carbon atom carries an —SR substituent, R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, or aralkynyl group that, optionally, includes at least one heteroatom in its carbon skeleton, the remaining available ring carbon atoms are optionally substituted, and said compound either:—(a) is more soluble in water at a temperature of 20-40° C.; (b) is less lipophilic; and/or, (c) has a greater therapeutic index; or; (d) is less soluble in water at a temperature of 20-40° C.; (e) is more lipophilic; and/or, (f) has a greater therapeutic index; than an equivalent cyclohex-2-en-1-one or cyclopent-2-en-1-one derivative in which a hydrogen atom replaces said —SR group.
CA2174327C Combination of progesterone antagonists and anti-oestrogens with partial agonistic action for use in hormone-replacement therapy for peri- and post-menopausal women This invention describes the use of at least one compound having a progesterone-antagonistic (PA) action and at least one compound having an antiestrogenic (A?) action with a simultaneous partial agonistic action for the production of pharmaceutical agents for hormone substitution therapy (HRT) for perimenopausal and postmenopausal women. In the case of combined use of progesterone antagonist and antiestrogen, the stimulation of the endometrium by the progesterone antagonist that is caused by its partial agonistic action when an antiestrogen is used by itself is inhibited. For example, a pharmaceutical agent according to the invention contains onapristone (progesterone antagonist) and tamoxifen (antiestrogen).
US20120276105 Use of cytokine expression to predict skin inflammation; methods of treatment Provided are methods for diagnosing the propensity of a subject to develop skin inflammation, in particular, psoriasis. Also provided are methods of treatment with antagonists of IL-17, IL-19, and/or IL-23.
US20100249747 Transdermal venous access locking solution Compositions and methods of employing compositions in flushing and coating medical devices are disclosed. The compositions include combinations of a chelating agent, anticoagulant, or antithrombotic agent, with a C4-C9 carboxylate antimicrobial agent, such as octanoic acid. Methods of using these compositions for coating a medical device and for inhibiting catheter infection are also disclosed. Particular combinations of the claimed combinations include, for example, octanoic acid or other C4-C9 carboxylate antimicrobial agent together with EDTA, EGTA, DTPA, heparin and/or hirudin in a pharmaceutically acceptable diluent.
WO2011050575A1 Hydroxy-substituted gold(iii) porphyrin complexes as histone deacetylase inhibitors A method for treatment of cancer by inhibiting the activity of histone deacetylase, comprising administering to a human in need of such treatment a composition containing a therapeutically effective amount of a gold(III) complex having the structural formula (I) of or a pharmaceutically acceptable salt thereof, wherein: - R is selected from the group consisting of -OH, -CH2OH, C2H4OH, -C3H6OH or C4H8OH; and - X is independently a pharmaceutically acceptable counter-ion.
EP2734213A2 Resorption enhancers as additives to improve the oral formulation of non-anticoagulant sulfated polysaccharides Aspects of the invention include methods for enhancing blood coagulation in a subject. In practicing methods according to certain embodiments, an amount of a non-anticoagulant sulfated polysaccharide (NASP) in combination with a gastrointestinal epithelial barrier permeation enhancer is orally administered to a subject in a manner sufficient to enhance blood coagulation in the subject. Compositions and kits for practicing methods of the invention are also described.
WO2009032668A3 2 -biphenylamino-4 -aminopyrimidine derivatives as kinase inhibitors The invention provides novel pyrimidine derivatives of formula (1) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF- 1 R) or anaplastic lymphoma kinase (ALK).
WO2007069053A1 Benzimidazole antagonists of the h-3 receptor This invention is directed to a compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula (I), a process of preparation of a compound of formula (I), a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), attention-deficit disorder (ADD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the G1 tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above.
CN103202821A Calcitriol soft capsules and preparation method thereof The invention provides calcitriol soft capsules with high bioavailability, high stability, convenience in administration, moisture absorption prevention, good sealing property and low price, which improves the bioavailability and the compliance of patients. In order to fulfill the aims, the calcitriol soft capsules and a preparation method thereof are finally obtained through a lot of experimental research; the calcitriol soft capsules comprise a soft capsule material and inclusion liquor, wherein the soft capsule material comprises gelatin, glycerol and water in a weight ratio of 10:3.5:9; and the inclusion liquor comprises calcitriol, co-emulsifier, oil phase and emulsifier in a weight ratio of (1-4): (30,000-35,000): (20,000-25,000): (80,000-100,000). The weight ratio of the soft capsule material to the inclusion liquor is 5:4.
US20080159987 Using bifidobacteria expressing rifamycin based non-sytemic antibiotic to treat nervous system disorders; probiotics Restless legs syndrome (RLS) is characterized by an urge for leg movement, often with abnormal leg sensations. Symptoms are triggered by rest, often at night, and improve temporarily with movement, especially walking. This syndrome has a prevalence ranging from 7% to 15% and significantly contributes to sleep disorders. A method of prevention of restless legs syndrome is disclosed that comprises orally administering a composition containing a therapeutically effective amount of rifaximin to a patient exhibiting symptoms of restless legs syndrome.
EP1294368A4 Management of snoring by oral administration of dimethyl sulfone A method of managing snoring is provided by the instillation orally of a solution containing 1-20 % methylsulfonylmethane by weight dissolved in water so as to cover the mucous membranes of the orophyrnx. Preferably, the solution has between 10 %-15 % by weight methylsulfonylmethane. The solution may be buffered, and/or a flavoring may be included. The method prefers that instillation occur as close to the sleep event as possible, and it should be at least within thirty (30) minutes to fifteen (15) minutes before a person retires for sleep. The solution may be introduced by spray or drop-wise, and a product packaging the solution in a suitable container is described.
CA2554874A1 Methods of reducing alcohol-induced dose dumping for hydromorphone sustained release oral dosage forms Disclosed are uses of sustained release hydromorphone dosage form that exhibit improved properties with respect to coadministration with aqueous alcohol.
CN101843617B Slow release preparation of compound Repaglinide-metformin hydrochloride The invention relates to a slow release preparation of compound Repaglinide-metformin hydrochloride and a preparation method thereof, which mainly solve the problem of the synchronous slow release of insoluble medicament Repaglinide and water-soluble medicament metformin hydrochloride. The preparation method uses hydroxypropyl methylcellulose, glyceride behenate, ethylcellulose and the like as framework materials and comprises the steps of: respectively pelletizing the Repaglinide and the metformin hydrochloride, pressing into bilayer tablets or respectively pressing into small tablets, and encapsulating into capsules. The prepared compound slow release preparation not only can improve the curative effect based on the complementation between medicament action mechanisms and decrease the dose of each individual component to reduce toxic or side effects of the medicaments, cut also can slow down the release of the medicaments, stabilize the blood concentration, reduce the administrationfrequency, and improve the compliance of patients.
US20120034193 Treatment of neurotrophic factor mediated disorders An agent selected from A/B-cis furostane, furostene, spirostane and spirostene steroidal sapogenins and ester, ether, ketone and glycosylated forms thereof is used to induce self-regulated homeostasis of neurotrophic factors (NFs), for example BDNF and/or GDNF, NFs with limited and manageable side effects in a subject, by modulating NFs in a non-toxic manner under homeostatic control. An effective amount of at least one such agent is administered to the subject, particularly in the treatment or prevention of a range of NF-mediated disorders, particularly neurological, psychiatric, inflammatory, allergic, immune and neoplastic disorders, and in the restoration or normalisation of neuronal and other function in or in relation to any damaged or abnormal tissue, including when assisting tissue (for example, skin, bone, eye and muscle) healing and general skin, bone, eye and muscle health.
US20100135956 Steroid modulators of progesterone receptor and/or glucocorticoid receptor The present invention relates to new steroid modulators of progesterone receptor activity and/or glucocorticoid receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
CN102209710A Pyrrolidines This invention relates to a class of pyrrolidine compounds of formula (I), and pharmaceutical ly acceptable derivatives thereof, to their use in med icine, to compositions containing them, and to processes for their preparation. It also relates to intermediates used in the preparation of such compounds and derivatives. In particular the compounds of formula (I) are useful for the treatment of EP2-mediated conditions, such as endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), chronic pelvic pain syndrome, polycystic kidney disease and polycystic ovarian syndrome.
US8492517 Melanocortin-1 receptor-specific cyclic peptides Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification, compositions and formulations including the peptides of the foregoing formula or salts thereof, and methods of preventing, ameliorating or treating melanocortin-1 receptor-mediated or responsive diseases, indications, conditions and syndromes.
WO2011000218A1 Compositions containing berberine or analogs thereof for treating rosacea or red face related skin disorders The present invention discloses topical pharmaceutical formulations of berberine and its biologically equivalent analogues, such as palmatine and coptisine, for the treatment of rosacea and other red face-related skin disorders. The topical pharmaceutical formulations of this invention contain purified berberine as the primary active drug ingredient at concentrations higher than 0.1%. The invention also discloses methods of treating rosacea and other red face related skin disorders, such as steroid-induced rosacea-like dermatitis, comprising the administration of topical pharmaceutical formulations that contain berberine or its biologically equivalent analogues, such as palmatine.
WO2014046589A1 Means and method for treating solid tumours In a cytotoxic compound of the general formula (I) R is H or methyl or methylene substituted by C1-C4 straight or branched alkyl, R1 is selected from the group consisting of H, C1-C4 straight or branched alkyl, methoxy, methoxy substituted by from one to three fluorine, halogen; R2 is H or C1-C4 straight or branched alkyl; X is CH or N; Y is CH or N.
CN102675370A Novel compound for curing cancer The invention discloses a novel compound for curing cancer. The novel compound is used for solving the problems of cancer curing. The chemical name of the compound is (4-(4-(4- methyl-3-(4-(pyridine-3-group) thiazole-2-amino group) carbaniloyl group) phenyl group) piperazidine-1-group) methyl sodium phosphate. An experiment shows that the novel compound is a tyrosine kinase inhibitor, has significant selective inhibition effects on epidermal growth factor receptor 2 in a vessel and vascular endothelial growth factor receptor (VEGFR) 3 and has significant inhibition effects on a plurality of nude mice xenograft such as colon cancer SW-620, ovarian cancer SK-OV-3, lung cancer Calu-3 and liver cancer.
CN101455648B Puerarin freeze-drying preparation The present invention relates to a lyophilized preparation of puerarin which is composed of lipidosome of cardiovascular drug puerarin and pharmaceutically acceptable carrier. The lipidosome of cardiovascular drug puerarin is composed of puerarin, lipidosome component, surfactant and freeze-drying supporting agent, wherein the weight ratio of puerarin, lipidosome component, surfactant and freeze-drying supporting agent is 1:50-40:0.1-1.5:0.1-1. The lipidosome component is dimyristica lecithin and cholesterol. The weight ratio between the dimyristica lecithin and cholesterol is 20-2:1. The surfactant is polysorbate-80. The freeze-drying supporting agent selects mannitol. The lyophilized preparation of puerarin of the invention has the advantages of high enveloping rate, good stability, excellent solubility, and evident reduced hemolytic adverse reaction of puerarin.
CN103316027A Application of catalpol and retinoic acid medicine composition in preparing medicine used for preventing or treating white matter damage The invention belongs to the field of medicine, and relates to the field of medicine preparation treatment activity. The invention specifically relates to a catalpol and retinoic acid medicine composition CAT-RA and an application thereof in preparing medicines used for preventing and treating with white matter damage after chronic cerebral ischemia. As a result of experiments of CAT-RA in cells and in chronic cerebral ischemia disease animal models, CAT-RA assists in reducing brain tissue inflammatory responses after brain damage, reducing white matter pathological changes, inhibiting oligodendrocyte apoptosis and myelin damage in white matters, and promoting oligodendrocyte precursor cell differentiation and maturation. CAT-RA has the effects of protecting white matters and promoting white matter remyelination. Therefore, CAT-RA can be used as an active component for preparing medicines used for preventing and treating white matter damage after chronic cerebral ischemia, and can also be used for preparing medicines used for treating other cerebral vascular related diseases characterized in white matter damages. The invention provides a novel solution for prevention and treatment of white matter damage related diseases.
CN103387596A Protopanaxadiol derivative and application thereof The invention discloses a protopanaxadiol derivative and pharmaceutically-acceptable salts, esters or solvates thereof. The protopanaxadiol derivative and the pharmaceutically-acceptable salts, esters or solvates thereof have a structure shown in the formula I. The invention further discloses application of the protopanaxadiol derivative and the pharmaceutically-acceptable salts, esters or solvates thereof in the preparation of drugs for treating and/or preventing tumors, particularly cervical carcinoma, leukemia, neuroblastoma, prostatic carcinoma, liver cancer and mammary cancer.
EP1379234B1 Halogenated aminobenzophenones and aminobenzoylpyridines as inhibitors of il-1 and tnf Compounds of formula I and pharmaceutically-acceptable and -cleavable esters thereof and acid addition salts thereof wherein the symbols are as defined are MAP kinase inhibitors, useful pharmaceutically for treating TNFα and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.
US20080125417 4-Tert-Butyl-N-(2-methyl-3-{2-[4-(morpholine-4-carbonyl)-phenylamino]-pyrimidin-4-yl}-phenyl)-benzamide;enzyme inhibitors of Burton's tyrosine kinase (Btk); autoimmune diseases; antiinflammatory/-arthritic agents; X-linked agammaglobulinaemia; antiallergens; osteoporosis; determining the presence Btk At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof, is described herein. Pharmaceutical compositions comprising at least one chemical entity of Formula 1, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
CN102887933A New compound and extraction method and application thereof The invention relates to a new compound and an extraction method and application thereof. The extraction method comprises the steps of pretreatment of pandanus tectorius raw medicinal material, extraction, separation, purification and the like. The new compound is subjected to qualitative identification and structural identification. According to the invention, the extraction and separation method is simple and quick and realizes high efficiency. A medicine prepared from the compound has the functions of dispersing wind and clearing heat and relieving summer-heat and promoting digestion, can be used for treating the fever and headache caused by external infection, dyspepsia and gassiness and dry throat and tongue, and can also be used for preventing influenza.
CN101690730A Method for quantum dot improvement and synchronous monitoring of antibacterial performance of ceftriaxone sodium The invention belongs to the technical field of biomedical and particularly relates to a method for the quantum dot improvement and synchronous monitoring of antibacterial performance of ceftriaxone sodium. Cadmium telluride quantum dots serving as inorganic nano material are added in merchant ceftriaxone sodium to improve the antibacterial performance of the merchant ceftriaxone sodium. Antibacterial experiments performed by taking Escherichia coli as an example indicate that the cadmium telluride quantum dots have a remarkable coordination and improvement effect, which is far better than those achieved by the single use of the cadmium and telluride, on the antibacterial performance of the ceftriaxone sodium. Meanwhile, the number of bacteria and medicament antibacterial performance are synchronously monitored by using the change in the fluorescence intensity of the mixed solution of ceftriaxone sodium and the cadmium telluride quantum dots in an antibacterial process. Thus, a foundation is laid for the effective judgment of the treatment course and withdrawal time of a medicament.
US20110008424 Sustained Release Solid Formulations and Methods of Manufacturing the Same Disclosed are a sustained release solid formulation comprising a drug, for example, oxycodone or its pharmaceutically acceptable salt, in a water-insoluble matrix, which comprises a wax type excipient and copovidone, and thus, has increased compressibility and fluidity and reduced adhesiveness, and a method of preparing the same.
US20110034476 Genetic polymorphisms and infertility Methods of screening for a cause of low sperm motility and/or for mitochondrial impairment in subjects are provided, comprising determining a genotype of the subject with respect to at least one choline metabolism gene and comparing the genotype of the subject with at least one reference choline metabolism genotype associated with low sperm motility and/or impaired mitochondrial function, wherein a similarity between the subject and reference genotypes indicates a cause of low sperm motility and/or impaired mitochondrial function in the subject. In another aspect, methods for treating subjects having low sperm motility and/or impaired mitochondrial function are provided, comprising administering to the subject an effective amount of a choline metabolism supplement composition to at least partially ameliorate the low sperm motility and/or impaired mitochondrial function.
EP2603587A1 Methods and pharmaceutical compositions for the treatment of hiv-1 infections The present invention provides methods and compositions (such as pharmaceutical compositions) for treating or preventing human immunodeficiency virus type 1 (HIV-1) infection. More particularly, the present invention relates to a blocking agent of a component of the purinergic signalling pathway selected from the group consisting of pannexin 1, ATP or P2Y2 receptor for use in the treatment or prevention of HIV-1 infection.
US20090269418 Compositions and Methods for Inducing Hair Growth Novel therapeutic methods and pharmaceutical compositions utilizing tellurium-containing compounds for inducing hair growth for the treatment of various types of alopecia and other conditions associated with hair loss.
US20120101088 Transmembrane Penetration Enhancer A transmembrane penetration enhancer includes a thermotropic liquid crystal suitably prepared for use in a therapeutic system to improve delivery of at least one active ingredient across a biomembrane and/or skin. The thermotropic liquid crystal comprises at least one cholesteryl ester and is effective in a mesomorphic state at a temperature of the biomembrane and/or skin. A therapeutic system includes the prepared thermotropic liquid crystal for enahanced transmembrane penetration and at least one active ingredient for delivery by the thermotropic liquid crystal. A method for making and using the transmembrane penetration enhancer is presented.
CN101412737A Anti-tumor bipyridine methyl substituted manganese amino acid complex, and preparation and application thereof The invention relates to a novel targeted antitumor small molecular compound and the technical field of preparation thereof, in particular to a targeted antitumor bipyridine methyl substituted aminophenol manganese composition, a preparation method and application thereof. Two new chiral bipyridine methyl substituted aminophenol compounds (L-model) and four new bipyridine methyl substituted aminophenol ligand manganese compositions are synthesized through a chemical method; and a structure of the composition is determined by a physical means. An in-vitro antitumor activity test researches the influence of the composition on tumor cells and finds out that the manganese composition with small lipin distribution coefficient has strong inhibiting function on the growth of the tumor cells of A549, Hela, HepG-2 and Eca109; and the manganese composition synthesized by the L-model compositions has stronger capacity for identifying the tumor cells. Data of an animal test of the manganese composition show that the composition has good tumor inhibiting function. The manganese composition and mitochondria have direct action; and the new manganese composition can be used as a new antitumor activity medical composition with the mitochondria as a target spot.
CN103027905A Use of arctigenin in preparing drug for treating synovitis The invention belongs to the field of medicines, and in particular relates to a use of arctigenin in preparing a drug for treating synovitis. The arctigenin preparation provided by the invention has a definite curative effect, a rapid effect and low toxicity in treating synovitis, is convenient to use, and has a good clinical application prospect.
CN103356549A Application of Sarcaboside A in medicine for treating or preventing oral ulcer The invention relates to an application of Sarcaboside A in preparing a medicine for treating or preventing oral ulcer. The application of the Sarcaboside A in preparing a medicine for treating oral ulcer is revealed for the first time; since a brand new skeleton type is adopted and the activity in treating oral ulcer is unexpectedly strong, the possibility of other compounds giving any prompt is avoided, and the Sarcaboside A has outstanding substantive features; and a remarkable progress is made in applying the Sarcaboside A to the treatment on oral ulcer.
US20080132551 Positive allosteric modulators of the nicotinic acetylcholine receptor The invention provides compounds of Formula I: wherein A, B, and X are described herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which α7 nAChR is known to be involved.
CN101607086B Compound bismuth composition and preparation method thereof The invention discloses a compound bismuth composition which contains antibiotics, a coated tablet of antibacterial agent and bismuth particle or powder, wherein the coated tablet is coated with Opadry II and the coating amount is 3 percent by weight; and the weight ratio of bismuth to the antibiotics to the antibacterial agent is 4-35:5-50:5-50. The invention also discloses a preparation method of the compound bismuth composition. The compound bismuth composition achieves good balance between the mutual action among active ingredients and the action of the active ingredients performed in stomach, and therefore is used for better eliminating the helicobacter pylori of stomach.
WO2009092133A1 Methods for identifying compounds capable of treating or preventing a diabetic complication via set7 or suv39 methyltransferases The present invention provides methods for identifying or designing compounds for the treatment or prevention of a complication of diabetes. The methods rely on the Applicant's identification of SET7 as a therapeutic target for these conditions.
CN103494819A Effect of camptothecin on rheumatoid arthritis Effect of camptothecin on rheumatoid arthritis. The invention relates to research of the immunosuppression effect of camptothecin on collagen-induced arthritis models, and the immunomodulatory effect of camptothecin on peripheral blood mononuclear cells of RA patients, and discusses the application of camptothecin to the treatment of rheumatoid arthritis. Experiments have confirmed that camptothecin can effectively inhibit arthritis, reduce bone destruction degree, and effectively relieve RA conditions.
CN102432483A Preparation method of acetyl levocarnitine hydrochloride, and drug application of acetyl levocarnitine hydrochloride The invention relates to a preparation method of acetyl levocarnitine hydrochloride, and drug application of the acetyl levocarnitine hydrochloride. The preparation method comprises the following steps of: (1) mixing acetic acid and levocarnitine base, and then stirring to prepare an acetic acid solution of the levocarnitine base, wherein the mass ratio of the acetic acid to the levocarnitine base is 1: 0.6 to 1.2; (2) mixing hydrochloric acid and acetyl chloride, and then stirring to prepare an acylation reagent, wherein the mass ratio of the hydrochloric acid to the acetyl chloride is 1: 2 to 4; and (3) mixing the acetic acid solution of the levocarnitine base and the acylation reagent, and performing acylation reaction to prepare the acetyl levocarnitine hydrochloride. The method is easy to operate and low in cost. Waste gas can be avoided. Drugs with the acetyl levocarnitine hydrochloride as an active ingredient are used for treating mechanical and inflammatory damages of peripheral nerve trunks or nerve roots with good effect.
EP2217250A2 Immunomodulating compounds and related compositions and methods Provided herein are compositions and methods for balancing a T-helper cell profile and in particular Th1, Th2, Th17 and Treg cell profiles, and related methods and compositions for treating or preventing an inflammatory condition associated with an imbalance of a T-helper cell profile.
US20100316727 Treatment of inflammatory disorders with ozone Methods for therapeutic treatment of inflammatory conditions in a mammalian patient provide clinical benefits including reduction of inflammation, vasorelaxation, reduction in edema and increased blood flow, the methods generally comprising extracorporeal treatment of blood, blood fractionate, or other biological fluid to expose such fluids to a precise, measured amount of ozone to produce a blood or biological fluid having a quantified absorbed dose of ozone, and reinfusing the treated biological fluid to the patient to provide therapeutic effects beneficial in the treatment of inflammatory disorders and related symptoms or conditions.
WO2012163291A1 Phenylpiperazine derivative for inhibiting tumor metastasis and tumor angiogenesis Disclosed are a phenylpiperazine derivative and pharmaceutically acceptable salts thereof, characterized in that the derivative has the structure as represented in formula (I); R1 in the formula is a -H, -R, -OR, -COOR, halogen, or -CN group, and R represents alkyl; the substitution of R1 on the benzene ring is at the para position, ortho position, or meta position of the piperazinyl; m is a natural number from 0 to 2; R2 is a substituted or unsubstituted carboxylic acid group or sulfonic acid group. The phenylpiperazine derivative and pharmaceutically acceptable salts thereof can be used in preparing medications for inhibiting tumor angiogenesis and tumor metastasis, in preparing tumor medications for treating liver cancer, breast cancer, ovarian cancer, stomach cancer, colon cancer, lung cancer, or melanoma, and in preparing auxiliary medications for tumor chemotherapy and surgery treatments.
US20110196017 Micro-rna that promotes vascular integrity and uses thereof The present invention relates to the identification of a microRNA, designated miR-126, that is a regulator of vascular integrity in endothelial cells. This endothelial cell-restricted microRNA mediates developmental angiogenesis in vivo, and targeted deletion of miR-126 in mice causes leaky vessels, hemorrhaging, and partial embryonic lethality, due to a loss of vascular integrity and defects in endothelial cell proliferation, migration, and angiogenesis. These vascular abnormalities resemble the consequences of diminished signaling by angiogenic growth factors, such as VEGF and FGF. These findings have important therapeutic implications for a variety of disorders involving abnormal angiogenesis and vascular leakage. Methods of treating disease states characterized by ischemia, vascular damage, and pathologic neovascularization by modulating miR-126 function are disclosed.
US20100291186 Transdermal Administration of Tamsulosin In an aspect of the invention, a composition for making a patch for the transdermal delivery of tamsulosin is provided. The composition comprises (a) at least about 1 wt % tamsulosin or a pharmaceutically acceptable salt of tamsulosin, (b) at least about 40 wt % polyisobutylene adhesive or hydrophobic synthetic rubber adhesive, (c) about 1-20 wt % of an aprotic solvent in which tamsulosin dissolves readily, (d) about 1-20 wt % of an unsaturated fatty acid or an alpha-hydroxy acid or a mixture of unsaturated fatty acids or alpha-hydroxy acids or of both unsaturated fatty acids and alpha-hydroxy acids, (e) a lipophilic permeation enhancer, and (f) a matrix modifier.
WO2008147373A3 Methods and compositions for reducing body weight using an estrogen fatty ester in an oil Compositions and methods for reducing the body weight of a subject are disclosed. The invention is directed to methods for reducing the body weight in a subject comprising administering therapeutically effective amounts of a fatty acid ester of an estrogen or estrogen derivative in an oil. Furthermore the invention is directed to compositions for reducing the body weight in a subject comprising administering therapeutically effective amounts of a fatty acid ester of an estrogen or estrogen derivative in an oil.
EP1139753B1 Formulations for treating disease and methods of using same A therapeutic mixture comprised of L-arginine and angiogenic growth factors is disclosed for the treatment of disease related to endothelial dysfunction. A schematic representation of NOS activation by select compounds and the conversion of L-arginine into NO is portrayed in the figure.
EP1767210A1 The medical use of paeoniflorin The present invention relates to the medical use of paeoniflorin with the following structure in treating and preventing nervous system diseases, such as apoplexy and Parkinson's disease, etc.
US7812178 such as (R)-3-(3-hydroxypyrrolidin-1-yl)-N-methyl-N-methoxypropanamide; poly(ADP-ribose)polymerase inhibitors The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.
US7462604 excellent stabilization effect at low temperature; no stickiness; Glycerin monopentadecanoate with 6-benzylaminopurine and/or the derivatives, polyglycerin fatty acid esters, sorbitan fatty acid esters A hair growth promotor which is an ethanol or aqueous ethanol preparation comprising, as active ingredients for a hair growth promotor, (A) at least one compound selected from fatty acids having a chain length of an odd number of carbon atoms, the derivatives of the fatty acids, aliphatic alcohols having a chain length of an odd number of carbon atoms and the derivatives of the aliphatic alcohols and (B) at least one selected from 6-benzylaminopurine and/or the derivatives thereof represented by the following Formula (I), wherein it further comprises (C) at least one of polyglycerin fatty acid esters and (D) at least one of sorbitan fatty acid esters: in Formula (I), R1 and R2 are defined. The hair growth promotor can have an excellent hair growth effect and can provide an excellent stabilization effect at low temperature and can provide good feeling having no stickiness.
EP1517701A2 Lewis y epitope-containing mucin fusion polypeptide vaccines, compositions and methods of use thereof The present invention provides compositions and methods for improving cancer vaccine immunogenicity using lewis Y modified mucin fused to a protein, in particular an immunoglobulin. The constructs can be produced by glycosylation of a protein, e.g. P-selectin glycoprotein ligand-1 (PSGL-1), with alpha 1,2 fucosyltransferase and alpha 1,3 fucosyltransferase.
US20100069295 Novel poly(ethylene oxide)-block-poly(ester) block copolymers The present invention relates to micelle-forming poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups on the polyester block therein. The biodegradability of these copolymers and their biocompatibilities with a large number of bioactive agents make them suitable as carriers for various bioactive agents. The bioactive agents, such as DNA, RNA, oligonucleotide, protein, peptide, drug and the like, can be coupled to the reactive groups on the polyester block of the copolymer.
US20120184612 Compositions and Methods Relating to Carotenoids A pet food composition having at least two carotenoids. The carotenoids can include a keto-carotenoid and at least one non-keto-carotenoid. The keto-carotenoid can include astaxanthin. The keto-carotenoid can include astaxanthin ester. The non-keto-carotenoid can include beta-carotene and/or lutein.
CN101961341A Application of glucose lowering function of mogrosides The invention discloses an application method of glucose lowering function of mogrosides (I, II, III, IV, or V, or mogrosides mixture). In the method, the mogrosides is prepared into drug, food and commodity with medical treatment and health-care functions to lead the content of the mogrosides to be 0.01-20% in the above products. The drug with the glucose lowering function of the invention can adopt the preparation in any form such as tablet, spray, powder, film agent and gels and the like. The food and the heath-care products with the glucose lowering function comprise chewing gum, beverage, tea, toffee and milk products. In the invention, the mogrosides is applied to a series of products lowering the glucose for the first time, while the previously developed mogrosides V product does not utilize glucose-lowering activity of the mogrosides. The glucose-lowering activity of the mogrosides is applied to human diabetes, hyperglycemia drugs, heath-care food and sweetener; and the mogrosides has wide prospect and important social and economic benefits.
CN101239094B Active component composition used as adjuvant drug for antitumor and preparation and application thereof Disclosed is an active component composition as an assistant drug for tumor, wherein an actual total content of astragalus polysaccharide and angelica polysaccharide which are active components reaches above 50% of total extracts. The active component capable of forming a suitable formulation with an appropriate physiologically acceptable excipient, can enhance the immune function and the disease-resistant ability, and also works as raw material for producing adjuvant treatment drug and rehab treatment drug after radiotherapy, chemotherapy and surgical treatment for tumor.
WO2008128832A1 Nitroderivatives of non-peptidic renin inhibitors for the treatment of cardiovascular, renal and chronic liver disease, inflammations and metabolic syndrome Non-peptidic renin inhibitors nitroderivatives of general formula (I) : A1- (Xa-ONO2) j wherein A1 is selected from the group consisting of formula (Ia), (Ib), (Ic), Id), (Ie) and (If). They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.
CN202777133U Aspirin enteric controlled-release preparation The utility model relates to an enteric controlled-release preparation, and in particular relates to an aspirin enteric controlled-release preparation. According to the preparation, a prepared aspirin controlled-release tablet is used as a tablet core; and a coat layer of an enteric coating covers an outer layer of the tablet core. In order to prevent mutual function of the aspirin and the enteric material in the tablet core, a corrosion-type isolating layer is covered between the tablet core and the enteric coating. After the aspirin is prepared to be the enteric controlled-release preparation, the interior of the stomach nearly does not release or is released a few, so that the release time in the intestines is greatly prolonged, a furious cracking and dissolution phenomenon is avoided in the intestines, the aspirin is stably released, the bioavailability is greatly improved, the degradation reaction of the aspirin which encounters the water is avoided, the dosage time is reduced, and the complaisance of a patient is improved.
CN101053581A External applied medicine for treating tympanitis and preparation method thereof A topical drug for treating tympanitis and its producing method belong to medicine technical field, which is used for treating the simple chronic suppurative otitis media with a project that: having the furazolidone 1.8-2.2, vitamin E 0.9-1.1, benne oil 25-65 as material, preparing, milling, mixing, bottling, then getting the topical drug liquid. The invention collects the treatment advantages of the chinese and foreign medicine to the local fester induced by bacillosis, selects the furazolidone, benne oil, vitamin E in proportion to produce topical drug for treating tympanitis, preferred chronic suppurative otitis media. Clinic application indicates that the drug is used for treating simple chronic suppurative otitis media and taking one time a day and working three day in a treatment period. It could properly prolong the treatment time with 100% efficiency to the patent with a long course of disease and a severe symptom. The invention also has a simple medication, a low toxic side effect, a low price, a strong patent compliance and etc.
WO2006051797A1 Therapeutic agent for interstitial cystitis A therapeutic agent for interstitial cystitis, characterized by containing a phenoxyacetic acid derivative represented by the following general formula (I): [Chemical formula 1] (I) (wherein R1 represents hydroxy or lower alkoxy) or a pharmacologically acceptable salt of the derivative. The phenoxyacetic acid derivative represented by the general formula (I) or pharmacologically acceptable salt or a hydrate or solvate thereof each functions to selectively stimulate a β3-adrenergic receptor and has remarkable inhibitory activity against a capsaicin-sensitive sensory nerve. They can hence be used as a preventive or therapeutic agent for interstitial cystitis and overactive bladder accompanied by a pain, other diseases in which a capsaicin-sensitive sensory nerve participates (e.g., acute or chronic, systemic or local pains or inflammation), irritable bowel syndrome (IBS), etc.
US20060004190 Glycoside and orthoester glycoside derivatives of apomorphine, analogs, and uses thereof Disclosed are glycoside and orthoester glycoside derivatives of apomorphine and analogs thereof to treat conditions and diseasessuch as erectile dysfunction.
CN101040937B Quality control method of Changyanning pills The invention discloses a method for preparing tablets for treating enteritis and its quality control method, wherein the tablets comprise creeping euphorbia 330-1120 parts, goldhair hedyotis herb 450-1530 parts, camphor root 330-1120 parts, nutgrass flatsedge rhizome 150-560 parts, maple leaves 150-560 parts and camphor 0.2-3 parts. The preparing process consists of disintegrating the raw materials, extracting with water, concentrating the water extract liquid at 80 Deg C. to a relative density of 1.05-1.35, granulating, drying and tabletting.
CN102232950A New application of rebeprazole in pharmacy The invention belongs to the technical field of medicine, and relates to a new application of rebeprazole in drugs for treating acute gastric mucosal injury caused by non-steroidal anti-inflammatory drugs and stress ulcer with bleeding.
WO2010082050A1 Macrocyclic and 7-aminoalkyl-substituted benzoxazocines for treatment of hepatitis c infections The present invention provides a compound of formula (I), wherein R1 is selected from hydrogen, hydroxyl, fluoro or a C1-4alkoxy group or R1 is linked to R3 to form a 4, 5 or 6-membered aliphatic ring optionally containing one N or O atom; R2 is selected from cyclopentyl or cyclohexyl optionally substituted by a fluoro; R3 is hydrogen or is linked to R1 as hereinbeforedefined; R4 is hydrogen, a C1-4alkyl group optionally substituted by a group NR8R9 in which R8 and R9 are each hydrogen or a C1-4alkyl group or R4 is linked to R6 to form a (CH2)mNR10SO2N group wherein m is an integer selected from 2 or 3 and R10 is a C1-4 alkyl group; R5 is hydrogen or a C1-4 alkyl group; R6 is hydroxyl or is linked to R4 as hereinbefore defined; R7 is hydrogen or an aliphatic ring of 4-7 ring atoms containing one or two heteroatoms selected from O, N or S or a group S(O), S(O)2,NH or NC1-4alkyl and optionally substituted by fluoro or R7 is a 5- 10-membered heteroaromatic ring system containing 1 to 4 heteroatoms independently selected from N, O and S, which ring is optionally substituted by one or two halo atoms or C1-4alkyl or C1-4alkoxy groups; Y is a single bond or a CH2 group; when R4 is linked to R6 and m is 3 then Y is a single bond; when R4 is linked to R6 and m is 2 then Y is a CH2 group; n is an integer from zero to four, with the proviso that when R1 is hydrogen, n is not zero; or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing it and its use in medicine, particularly for the treatment of HCV infections. Hepatitis C (HCV) is a cause of viral infections. Methods of preparing compounds of the formula (I) arc also disclosed.
WO2012173219A1 Novel biaryl ether derivative The present invention relates to a compound having an excellent DGAT inhibitory activity and an excellent antifeeding activity or a pharmacologically acceptable salt thereof. A compound represented by general formula (I) [wherein R1 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group or a C3-C6 cycloalkyl group; R2's independently represent a halogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group or a hydroxy group; and n represents an integer of 0 to 2] or a pharmacologically acceptable salt thereof.
CA2440160C Antitumor compositions containing taxane derivatives A pharmaceutical composition comprised of acetocyclorpropyl taxotere or a derivative thereof, and at least one of an alkylating agent, an antimetabolite, a spindle poison, an epidophyllotoxin, an antibiotic, and enzyme, a topoisomerase inhibitor, a plantinum coordination complex, a biological response modifier or a growth factor inhibitor is described.
US20110195924 Methods of Inhibiting the Interaction Between S100P and the Receptor for Advanced Glycation End-Products A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, and/or other analogs, or salts, hydrates, or solvates thereof. In addition, provided herein are methods of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, and/or other analogs, or salts, hydrates, or solvates thereof.
CN103417535A Amoxicillin potassium clavulanate tablet and method for preparing same The invention discloses an amoxicillin potassium clavulanate tablet. In the tablet, the weight ratio of amoxicillin and potassium clavulanate is 4-8:1. The tablet is formed by even mixing of medicated granules, the potassium clavulanate, a disintegrating agent and a lubricating agent in a direct tablet compressing mode, wherein the disintegrating agent is dried to have the moisture content lower than 3%. The medicated granules comprise amoxicillin and tartaric acid, wherein the weight ratio of the amoxicillin and the tartaric acid is 1:0.1-0.5. The tablet is rapid in dissolution, good in stability, few in auxiliary material kind and simple in preparation technology.
US20120064136 Anti-aging and wrinkle treatment methods using nanoemulsion compositions The present invention relates to methods for treating, preventing, minimizing, and/or diminishing signs of aging in the skin comprising administering to the subject in need thereof a nanoemulsion composition.
CN101987088A Preparation and applications of paeonol controlled-release preparation The invention relates to a preparation and applications of a paeonol controlled-release preparation in the technical field of the medicine. The paeonol controlled-release preparation refers to a group of controlled-release and long-time effective preparations which contain the microspheres and gel matrix tablets used for preparing tablets or capsules, and thermosensitive in situ gel for external use, wherein the specifications of the prepared paeonol controlled-release preparation are 60mg and 120mg; under special conditions, the accumulative release rate at 2h is less than 20% of the labeled amount, the accumulative release rate at 6h is 40-60% of the labeled amount and the accumulative release rate at 12h is more than 80% of the labeled amount respectively; and the paeonol controlled-release preparation can be used to cure rheumatoid arthritis. By using the thermosensitive in situ gel for external use, the preparation residence time of the affected part can be significantly prolonged.
CN101317947A Drinking particle for taking a tonic to build up health for confinement The present invention relates to a granule for tonify in post-partum period. The present invention is characterized in that: radix astragali, Chinese date, radix codonopsitis, honey, white chrysanthemum, lily, motherwort and Pu'er tea, and the like, are used for extracting a condensed extract which is dried and ground, evenly mixed with brown sugar by stirring, then pelletized, dried, and sterilized, thus obtaining the granule.
EP1698696A1 Target protein of antidiabetic agent and novel antidiabetic agent insuful corresponding thereto The present invention is intended to elucidate a molecular target of an antidiabetic such as a thiazolidine derivative. The present invention provides a screening method for an antidiabetic, comprising the steps of: bringing a candidate substance to be screened into contact with a protein represented by the following (a) or (b): (a) a protein comprising the amino acid sequence represented by SEQ ID NO: 2; or (b) a protein comprising an amino acid sequence derived from the amino acid sequence represented by SEQ ID NO: 2 with the deletion, substitution, addition, or insertion of one or plural amino acids and interacting with the antidiabetic; and detecting the interaction between the candidate substance and the protein.
CN1883475A Compound teribinafine hydrochloride solution for animal The invention discloses a compound terbinafine hydrochloride solution for animals, which is prepared mainly from terbinafine hydrochloride, Metronidazole, thiabendazole and cypermethrin. The solution has substantial effect in treating pet granuloma skin diseases.
US20110165067 Carbohydrate functionalized catanionic surfactant vesicles for drug delivery Carbohydrate functionalized catanionic vesicles that include a glycoconjugate and/or peptidoconjugate for vaccination or drug delivery, methods for forming these, and methods of using these.
US20120178739 Lactam compounds useful as protein kinase inhibitors The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
CA2845007A1 Noribogaine salt ansolvates Stable noribogaine salt ansolvates are useful for preparing pharmaceutical compositions and for alleviating nociceptive pain in a patient. Such ansolvates can be prepared by slurrying solvated forms, preferably MeOH solvated noribogaine hydrochloride in EtOH/water.
US20080207592 Novel 1,4-benzothiazepine-1,1-dioxide derivative having improved properties, method for the production thereof, medicaments containing said compound, and use thereof The invention relates to the compound of the formula (A) and also to its physiologically acceptable salts. The compound is suitable as, for example, a hypolipidemic.
US20120121725 Cosmetic composition for the treatment of acne comprising a peptide extract of schizandra The present invention relates to a cosmetic, nutraceutical or dermatological composition for treating or preventing acne, comprising a peptide and oside extract of Schizandra fruit and a suitable excipient. Preferably, the extract is obtained from Schizandra sphenanthera. The composition may also comprise at least one anti-acne agent selected from a sebum-regulating agent, an antibacterial and/or antifungal agent, a keratolytic agent and/or a keratoregulating agent, an astringent, an anti-inflammatory and/or anti-irritant, an antioxidant and/or a free-radical scavenger, a cicatrizing agent, an anti-ageing agent and a moisturizing agent. The invention also relates to a method for cosmetic treatment of acne, characterized in that a cosmetic composition according to the invention is applied to the affected areas of the skin, or in that the affected individual takes a nutraceutical composition according to the invention orally.
CN101948887A Preparation method and application of recombinant phycocyanobilin The invention discloses a method for preparing recombinant phycocyanobilin, in particular a method for producing the recombinant phycocyanobilin by gene engineering technology. The method comprises the following steps of: cloning phycocyanobilin synthesizing key enzyme genes (hol and pcyA) from algae and cloning the key enzyme genes to proper expression vectors; inoculating a recombinant vector into an Escherichia coli expression system for heterogenous expression, and synthesizing the recombinant phycocyanobilin through enzymatic catalytic reaction; and finally performing extraction, chromatography and other purification steps to prepare the recombinant phycocyanobilin. The prepared recombinant phycocyanobilin has the advantages of higher capacity of removing DPPH radicals, can be used for treating a plurality of diseases caused by oxidative damage, and also can be used as an additive in functional foods.
CN1759858A Prescription of compound unique oil drop pills and preparation method A dripping pill of lamiophlomis herb for acesodyne is prepared from the extract of lamiophlomis herb borneol and proper matrix through proportional preparing. Its advantages are unique preparing process and high curative effect.
CN103656643A Application of p38-STAT1 (Signal Transducer and Activator of Transcription 1) signal path conditioning agent to preparation of product for controlling HTRA1 (High Temperature Requirement A1) expression The invention provides an application of a p38-STAT1 (Signal Transducer and Activator of Transcription 1) signal path conditioning agent to the preparation of a product for controlling HTRA1 (High Temperature Requirement A1) expression. The p38-STAT1 signal path conditioning agent comprises an agonist and an inhibitor, wherein the agonist is an interferon-gamma and/or anisomycin and an analogue thereof, and the inhibitor is a phosphokinase p38 inhibitor or STAT1 inhibitor; the phosphokinase p38 inhibitor is SB203580 and an analogue thereof, or the STAT1 inhibitor is an MTA (Methylthioadenosine) and an analogue thereof; and a serine protease HTRA1 is related to inflammatory diseases and related diseases thereof or diseases related to the formation or migration of tumors. Therefore, the invention develops a novel HTRA1 gene expression control method to treat HTRA1 related diseases and provides a novel application of the p38-STAT1 signal path conditioning agent, and the p38-STAT1 signal path agonist can be used for inhibiting the expression of the serine protease HTRA1 so that the HTRA1 related diseases are treated.
US7253254 Polypeptide variants with increased heparin-binding capacity The invention pertains to polypeptide variants with increased heparin-binding ability. Increased heparin-binding ability is achieved by addition, insertion, and/or substitution of an amino acid sequence X1X2X3X4X5X6 (SEQ ID NO. 1 or NO.2). Polypeptide variants according to the invention are particularly suited for stimulation of chondrogenesis, osteogenesis, and wound healing. The invention also pertains to amino acid molecules that encode said polypeptide variants, host cells containing said nucleic acid molecules, and processes for producing the polypeptide variants.
WO2014056953A1 Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases This invention concerns pyrrolo[3,2-d]pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treatment and /or therapy of diseases.
US20110091417 Interleukin-22 Polypeptides, Nucleic Acids Encoding The Same And Methods For The Treatment Of Pancreatic Disorders The present invention is directed to interleukin-22 polypeptides and nucleic acid molecules encoding those polypeptides. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention.
US20080318901 enhancing wound repair; treating reperfusion type injury; lyso-lipid phosphate phosphatase inhibitor; phosphoric acid mono-[3-(4-phenyloxy-pyrimidine)-2-octadec-9-enoylamino-propyl] ester or salt The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
EP1933847A1 Carotenoid analogs or derivatives for the inhibition and amelioration of inflammation A method for inhibiting and/or ameliorating the occurrence of diseases in a human subject whereby a subject is administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative. In some embodiments, the administration of analogs or derivatives of carotenoids may inhibit and/or ameliorate the occurrence of diseases in subjects. In some embodiments, analogs or derivatives of carotenoids may be water-soluble and/or water dispersible. Maladies that may be treated with analogs or derivatives of carotenoids embodied herein may include diseases that provoke or trigger an inflammatory response. In an embodiment, asthma may be treated with analogs or derivatives of carotenoids embodied herein. In an embodiment, administering analogs or derivatives of carotenoids embodied herein to a subject may control or affect the bioavailability of eicosanoids. In an embodiment, atherosclerosis may be treated with analogs or derivatives of carotenoids embodied herein. In an embodiment, administering the analogs or derivatives of carotenoids embodied herein to a subject may control or affect the bioavailability of 5-LO-catalyzed eicosanoid metabolites. In an embodiment, 5-LO-catalyzed eicosanoid metabolites that may be controlled or affected by administering analogs or derivatives of carotenoids to a subject may include proinflammatory effector molecules (e.g., leukotrienes).
WO2011074660A1 Elution-stabilized preparation Disclosed is a solid preparation which does not undergo the delay of elution of an active ingredient thereof even after the storage for a long period. Specifically disclosed is a teneligliptin-containing solid preparation which contains teneligliptin, a salt thereof or a solvate of teneligliptin or the salt in an amount 1.5- to 10-fold larger than the content that is desired to be contained in a solid preparation and which contains a teneligliptin-containing part in a separated form.
CN103189069A Treatment of neurodegenerative diseases by targeting miRNA The present invention relates to a pharmaceutical composition for preventing or treating neurodegenerative diseases by targeting a specific miRNA. In addition, the present invention relates to a kit for diagnosing neurodegenerative diseases. A miR-206 target found in the present invention, which is highly expressed in both animal models of Alzheimer's disease and human brain samples, is a substantial treatment target selected without artifact errors. An antisense oligonucleotide of the present invention as an inhibitor for miR-206 suggests a successful result in treatment of neurodegenerative diseases by targeting miRNA. The antisense oligonucleotide of the present invention inhibits the function of miR-206 to greatly increase the levels of BDNF and IGF-1 and to increase the regeneration of synapses, thereby treating neurodegenerative diseases, particularly Alzheimer's disease.
WO2008012089A8 Polyphenol/peptide composition and use thereof for promoting gastric health The present invention relates to a composition which comprises a first component from the group of the polyphenols and a second component from the group of the lactic peptides. Furthermore, the invention relates to a process for the preparation of the composition and to the use of the composition for the preparation of products which are used either as pharmaceuticals or as dietetic foodstuffs.
EP1268396B1 Diphenyl ether compounds useful in therapy A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein R3 is independ ently CF¿3?, OCF3, C1-C4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and the other variables are as defined in the claims. These compounds inhibit monoamine re-uptake and in particular exhibit activity as selective serotonin re-uptake inhibitors. They are useful in disorders such as depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder, substance abuse disorders and sexual dysfunction including premature ejaculation.
CN101347598A Liniment spray for bonesetting and pain-alleviating By applying motherland medical theory and combining personal over thirty-year practical experience, the invention relates to a pure Chinese drug preparation which is prepared by developing the precious experience of the motherland herbal medicine and researching with great concentration, in particular to a bone setting stab spraying liniment having strict, reasonable and optimal matched formula. The bone setting stab spraying liniment has obvious healing efficacy on cervical spondylosis, lumbar vertebrae disease, various acute and chronic sprain, wind cold-dampness, rheumatism, hyperosteogeny, all sorts of joint diseases and various closed fracture, etc. After the bone setting stab spraying liniment is used by 868 patients clinically according to the period of treatment, the total effective rate is 99.8%. The bone setting stab spraying liniment is characterized by quickly relieving pain, easing the pain symptom within a few minutes to be disappeared, rapid absorption, being free from contamination, non-toxicity, no stimulation, no side effect and convenient use, and is an ideal external medicine specially used for treating the diseases such as bone fracture, neck, shoulder and lumbocrural pain and arthrodynia.
EP0853618B1 Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) n- (aminoiminomethyl)phenylalkyl -azaheterocyclylamide compounds The compounds of formula (I) exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula (I), compositions containing compounds of formula (I), and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
US7531556 Compositions useful as inhibitors of rock and other protein kinases The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
WO2007009688A1 Thiocarbonyl-substituted pyrazoline compounds, their preparation and use as cb1 modulators The present invention relates to thiocarbonyl-substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
CN1857213A Slow released anticancer injection with both antimetabolite and cellular poison medicine The slow released anticancer injection consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material carrier, and the solvent is special solvent containing suspending agent. The effective anticancer component is antimetabolite Nolatrexed, Carmofur, etc and/or cytotoxic medicine selected from Camptothecin, Docetaxel, Oxaliplati, etc. The slow releasing supplementary material is selected from difatty acid-sebacic acid copolymer, poly(erucic acid dipolymer-sebacic acid), poly(fumaric acid-sebacic acid), EVAc, etc. The suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for raising the effect of chemotherapeutic medicine, radiotherapeutic medicine, etc.
CN102973575A Application of cryptotanshinone in preparing drug used for treating psoriasis The invention discloses application of cryptotanshinone in preparing a drug used for curing psoriasis. The drug contains a therapeutically effective amount of cryptotanshinone and a pharmaceutically acceptable vector, wherein the content of the cryptotanshinone is 1-99 percent by weight. The cryptotanshinone is prepared into clinically or pharmaceutically acceptable dosage forms including an oral solid preparation such as a capsule and a tablet, or an external preparation such as an emulsifiable paste, a cream and a gel, is applied to patients who need to be cured in external and oral ways, plays an obvious role in restraining HaCaT cell proliferation, and can be used for preparing the drug used for curing psoriasis. Animal experiments and clinical tests prove that the cryptotanshinone has the beneficial effects of obvious effect, good safety and higher development prospect and is a novel drug used for treating psoriasis.
US20090274746 Methods and compositions for controlled delivery of phytochemical agents The presently-disclosed subject matter provides compositions and methods for treating a cancer by providing a composition comprising a biocompatible polymeric matrix incorporating an effective amount of a phytochemical agent, a combination of phytochemical agents, or a phytochemical agent and a chemotherapeutic agent. Further, provided is a device for uterine cervical insertion for local delivery.
WO2005020974A1 Novel use of a polyamine-poor composition for the production of a medical human food The invention relates to a novel use of a food composition for human use, having fewer than 1600 picomoles of polyamines, for the production of a medical food which is intended to combat a syndrome or pathology involving N-methyl-D-aspartate receptor subunit NR2-B.
CA2811171A1 Quinazolin-4 (3h) -one derivatives used as pi3 kinase inhibitors The present invention relates to the compound of formula (I) and to compositions comprising the same and to the use of the compound and to compositions of the compound in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the said compound.
US20120065236 Methods for concomitant treatment of theophylline and febuxostat The present disclosure relates to a method of treating hyperuricemia in a patient that also suffers from a second disease state requiring treatment with theophylline, wherein the patient receives concomitant treatment with a xanthine oxidoreductase inhibitor and theophylline without resulting in theophylline toxicity to the patient and without substantial adjustments to the manufacturer's recommended dosage of theophylline.
WO2008105392A1 3-amino-2-indolylbutyrolactam derivative, process for production of the same, and pharmaceutical agent comprising the same as active ingredient Disclosed is a substance for inhibiting cell death, which is effective as a prophylactic or therapeutic agent for the progress of a condition of a disease whose of progress or exacerbation is associated with cell death. Specifically disclosed are: a compound represented by the general formula (1) and a pharmaceutically acceptable salt thereof; and a use application associated with a cell death-inhibiting activity of the compound.
US20080153815 Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors Pinane-substituted pyrimidinediamine derivatives derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or conditions associated with Axl catalytic activity are also disclosed.
US20050245466 Use of topoisomerase inhibitors and heat shock protein 90 inhibitors for use in chemotherapy The present invention relates to the use of a first agent that attenuates topoisomerase II (Topo II) activity and a second agent that inhibits Heat Shock Protein 90 (HSP90) for use in chemotherapy. The agents are particularly useful in the treatment of cancer and destruction of micro-organisms. The invention also relates to screening methods, diagnostic methods and methods for evaluating or monitoring chemotherapy regimens.
CN101311176A Isoquinoline compounds, preparation method and use thereof The invention discloses a novel isoquinoline compound, and a synthetic method thereof as well as an application of the compound, which is used as an agonist or an inhibitor of dopamine receptors in the medicines for treating Parkinson's disease, schizophrenia, tristimania, Tourette syndrome, attention-deficit hyperkinetic syndrome, pituitary tumor, etc. The constitutional formula of the compound is as follows: wherein, R1 is the hydrocarbyl with a H, C1-C10 linear chain or fork chain, heteroatom-substituted hydrocarbyl and aromatic or fatty heterocycle or non-heterocycle substituted alkyl; X is carbonyl, methylene and imidogen, and is more than C-OH or more than C=; Y is carboxide, methylene and imidogen, and is more than C= or more than C=N-OH; the compound can have no D cycle or the D cycle can be various heterocycles of substituted five-membered fat and substituted six-membered fat or substituted five-membered aromatic and six-membered aromatic; n is 0-3.
CN103040833A Pharmaceutical composition of voriconazole and preparation method The invention provides a pharmaceutical composition of voriconazole and a preparation method. The composition mainly comprises voriconazole, polyethylene glycol melting agent 6000 and other auxiliaries. The preparation method comprises the steps of uniformly mixing the voriconazole with various auxiliaries, preparing medicament particles by using a hot-melting granulation technology, pressing the particles to be tablets and coating.
EP1038524B1 L-threonate ferrous, as well as pharmaceutical composition and use for improving and treating human anemia thereof The present invention provides L-threonate ferrous shown by formula (I), as well as pharmaceutical composition thereof. L-threonate ferrous may be useful to mammal, in particular human body for supplementing iron to improve and treat nutritional, posthemorrhagic anemia and hemolytic blood.
CN101012224A Quinoline derivative, preparation method and medical use thereof The invention discloses a making method of compound I and drug composition and application to treat tumour, which is 3-nitrile quinoline derivant (I) as dual-inhibitor protein kinase of tyrosine and nitric oxide synthase, wherein G1, G2, G3, G4, X, Z and n are defined as instruction.
WO2013030058A1 Use of diclofenac The invention relates to a previously unknown indication of the active ingredient diclofenac which has been known for a long time, in particular to a use of diclofenac including the physiologically tolerable salts thereof for the prophylaxis and therapy of influenza infections and of the disease symptoms caused by influenza infections. The use of diclofenac, according to the invention,makes it possible to treat, in a highly effective manner, the plurality of symptoms of an influenza infection using a single, well-known, active ingredient which has few adverse effects. The therapeutic use of diclofenac, according to the invention, also helps to prevent the pertinent disease symptoms of influenza infections from occuring in the first place, and consequently, the common cold infections have a mild course. Moreover, the onset of an influenza infection can be largely prevented by the prophylactic administration of diclofenac.
US20080260748 Desmocollin 2 (DSC2) specific immunoglobulin for use in prevention and treatment of cell proliferative disorders The present invention is based on the discovery that the cytoxicity of anti-desmocollin 2 (DSC2) antibodies can be used for treating various cancers including lung, colon, pancreatic, prostate, breast, gastric or liver cancers. Specifically, the present invention provides antibodies against DSC2 that have effector function. Furthermore, the present invention provides methods and pharmaceutical compositions that comprise anti-DSC2 antibody as an active ingredient for damaging DSC2-expressing cells via the effector function of the antibody.
WO2013143319A1 Quinazoline derivative and usage thereof The present invention provides a quinazoline compound shown in formula (I), or pharmaceutically acceptable salt thereof. R1, R2 and R7 are independently and respectively selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, halogenate C1-6 alkyl, halogenate C1-6 alkoxy, hydroxyl C1-6 alkyl, hydroxyl C1-6 alkoxy, C1-6 alkoxy C1-6 alkoxy, C3-8 cycloalkyloxy, optional aryl or heteroaryl substituted by R6, nitryl, amino, C1-6 alkylamino, and di(C1-6 alkyl)amino; it comprises at least one C3-8 heterocycloalkyloxy selected from N, O, S heteroatoms; Z is -NR4-, C(R5)2, S or -O-, R4 being hydrogen or C1-3 alkyl, and R5 being selected from hydrogen or C1-3 alkyl; R3 is selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy or halogenate C1-6 alkyl; R6 is selected from hydrogen, C1-3 alkyl, hydroxyl, halogen, C1-3 alkoxy; and n is 0 to 5. The present invention further provides a preparation method of the compound shown in formula (I) or the pharmaceutically acceptable salt and pharmaceutical usage thereof, which can be used as medicines or lead compounds for curing diseases such as tumour and cancer related to protein tyrosine kinase.
US20120095108 Composition containing microbial zeaxanthin and preparation thereof The present invention relates to a composition for prevention and/or treatment of human skin alteration or disease comprising an extract of marine bacteria selected from Flavobacteriaceae, wherein the extract contains an effective amount of zeaxanthin. The present invention also relates to a method for preparing the above composition, comprising: (a) culturing marine bacteria selected from Flavobacteriaceae, more specifically, from Olleya marilimosa, in a liquid culturing medium to form pigments containing zeaxanthin; (b) separating cell mass of the marine bacteria with the pigments and the liquid culturing medium and collect the cell mass to obtain the above composition, and (c) optionally mixing the cell mass and a carrier.
CN103340855A Compound amoxicillin and clavulanate potassium tablet and preparation method thereof The invention relates to a compound amoxicillin and clavulanate potassium tablet and a preparation method thereof. The tablet consists of the following components in percentage by weight: 15 to 30 percent of amoxicillin, 5 to 15 percent of a clavulanate potassium mixture, 30 to 65 percent of a filler, 1.5 to 8 percent of crosslinked povidone, 0.6 to 3 percent of povidone K30, 1 to 3 percent of silica and 1 to 5 percent of glyceryl behenate. The preparation method comprises the following steps: adding the amoxicillin, the filler and the crosslinked povidone into a pelletizer, mixing and adding an adhesive in a mixing process; and adding the prepared amoxicillin granules and clavulanate potassium mixture, the silica and the glyceryl behenate into a mixing machine, mixing, discharging and tabletting. Although the compound amoxicillin and clavulanate potassium tablet adopts a half-wet method to pelletize, the clavulanate potassium is unlikely to degrade, so that the stability of a medicine is guaranteed effectively.
US20110064785 Nanostructure-Enhanced Platelet Binding and Hemostatic Structures Methods, systems, and apparatuses for nanomaterial-enhanced platelet binding and hemostatic medical devices are provided. Hemostatic materials and structures are provided that induce platelet binding, including platelet binding and the coagulation of blood at a wound/opening caused by trauma, a surgical procedure, ulceration, or other cause. Example embodiments include platelet binding devices, hemostatic bandages, hemostatic plugs, and hemostatic formulations. The hemostatic materials and structures may incorporate nanostructures and/or further hemostatic elements such as polymers, silicon nanofibers, silicon dioxide nanofibers, and/or glass beads into a highly absorbent, gelling scaffold. The hemostatic materials and structures may be resorbable.
CN103083328A Preparation method of rape bee pollen long chain fatty acids and derivatives thereof The present invention discloses a preparation method of rape bee pollen long chain fatty acids and derivatives thereof. The preparation method comprises the following steps: a) providing an extract of rape bee pollen after washing and centrifuging; b) using microwave to vacuum dry the extract; c) conducting supercritical fluid extraction to obtain a supercritical extract; d) extracting the supercritical extract with C1-C5 alcohols or aqueous solutions thereof to get rape bee pollen long chain fatty acids and the derivatives thereof. The preparation method of rape bee pollen long chain fatty acids and derivatives thereof is high in controllability, low in energy consumption, low in pollution and low in cost, and is suitable for industrial production.
CN101817861A Method for preparing high-purity astragaloside for treating diabetes nephropathy and peripheral neuritis of diabetes complications The invention relates to a method for preparing high-purity astragaloside for treating nephropathy and peripheral neuritis of diabetes complications. A monomer compound system is obtained from astragalus root. The method comprises the following steps of: extracting an astragalus medicinal material serving as a raw material by using ethanol hot refluxing, performing alkaline hydrolysis on extract, absorbing macroporous resin, collecting eluant at certain alcohol concentration, and performing silica gel purification, recrystallization and other technical processing to obtain an astragalus pure product. The purity of the astragaloside prepared by the method reaches between 98 and 100 percent. The astragaloside prepared by the method is a preparation prepared from active ingredients; pharmacological experiments show that the high-purity astragaloside can effectively treat nephropathy and peripheral neuritis of diabetes complications. The method has the advantages of simple and convenient operation, high product purity, high yield, low production cost, no pollution and the like.
CN102091121A Health-care product for nourishing five internal organs and curing impotence and prospermia and preparation method thereof The invention discloses a health-care product for nourishing five internal organs and curing impotence and prospermia and a preparation method thereof. The health-care product comprises the following raw materials: cordyceps, Chinese angelica, soybean and the like; and the raw materials are processed by immersing and other processes to form the health-care product for nourishing the five internal organs and curing the impotence and the prospermia with formulations such as powder, capsules, tablets, oral liquid preparations and the like which are suitable for oral administration. The invention has the advantages that the health-care product has the effects of tonifying heat, lung, liver, spleen and kidney, strengthening the body, enhancing the functions of reproductive organs and causing and enhancing sexual desire directly, and has the obvious rehabilitation and health-care effects on angina, stomachache, lumbago, prostatitis, impotence, prospermia, female coital excess, frigidity and the like, does not have the side effect during moderate coitus and has an adverse reaction during acolasia.
CN102580054A Female scalp soothing hair-care shampoo and preparation method thereof The invention discloses a female scalp soothing hair-care shampoo and a preparation method thereof. The female scalp soothing hair-care shampoo comprises hydrolytic lupin protein, radix salviae miltiorrhizae extract, mulberry leaf extract, ginseng root extract, fleece-flower root extract, tetrahydro-piperine, ethanol, butylene glycol and water. The female scalp soothing hair-care shampoo can directly permeate into the hair follicle deep layer, so that the hair follicles obtain sufficient nutrients; the female scalp soothing hair-care shampoo can inhibit excessive secretion of sebaceous glands and improve the grease embolus in the follicular orifices; the female scalp soothing hair-care shampoo can promote the scalp blood circulation, increase the blood flow and improve the hair growth environment; and thus, the alopecia can be quickly controlled, and the female scalp soothing hair-care shampoo can nourish the hair, keep the scalp clean and dry, relieve the tension of scalp and promote the healthy growth of hair.
EP1852433B1 Carbazole derivative, solvate thereof, or pharmaceutically acceptable salt thereof A novel carbazole derivative which has the excellent functions of reducing the weight of fat tissues and lowering the blood sugar level and the blood lipid level. It is useful as a preventive/therapeutic agent for fatty liver, obesity, lipid metabolism abnormality, visceral fat, diabetes, hyperlipemia, impaired glucose tolerance, hypertension, non-alcoholic fatty liver, or non-alcoholic steatohepatitis. It is a carbazole derivative represented by the following general formula (I). (In the formula (I), ring A represents phenyl, etc.; X represents -O-, etc.; Y represents =N-, etc.; a and b each represents methylene, etc.; V and Z each represents -O-, etc.; W represents C1-10 alkylene in which one or two hydrogen atoms may be replaced with phenyl or C1-5 alkyl, or represents 1,2-phenylene, 1,3-cyclohexyl, etc.; R1 represents methyl, etc.; R2 represents methoxy, etc.; and R3 represents carboxy, etc.)
CN102603637A Pyrazol compound and purpose of pyrazol compound used as receptor tyrosine kinases (RTK) and phosphatidyl inositol 3-kinase (PI3K) dual inhibitors The invention provides a group of novel tyrosine kinase and phosphatidyl inositol 3-kinase (PI3K) dual inhibitors, which have higher anti-tumor activity. A preparation method for synthesizing the novel tyrosine kinase and PI3K dual inhibitors is characterized in that the novel tyrosine kinase and PI3K dual inhibitors are obtained through manual synthesis. The novel tyrosine kinase and PI3K dual inhibitors synthesized by using the method provided by the invention can be used for preparing cancer treatment medicine.
US20050009851 Use of cyclopeta[g]quinazoline derivatives for treating cancer Cyclopenta[g]quinazolines of the formula (I): wherein; A is hydrogen or a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C1-4 alkenyl, C1-4 alkynyl, C2-4 hydroxyalkyl, C1-4 halogenoalkyl or C1-4 cyanoalkyl, or R0 and R1 together with the intermediate N form a five- or six-membered heterocyclic ring, p is an integer in the range 1 to 4; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediy which may optionally bear one or two subtituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and R3 is a group the following formula: (II) and pharmaceutically acceptable salts or calers may be used in the treatment of solid tumours.
US6878826 Perfluoronated cycle-containing tertiary amines used as a basis for gas-conveying emulsions and device for the production thereof Tertiary perfluorocycloamines (TPFCAs) of general formula (1) where n=1 or 2, m=2 or 3, X is wherein at n=2 X is as the basis for gas transport emulsions. TPFCAs comprise a group of compounds which are close in their physicochemical properties to perfluoro-N-(4-methylcyclohexyl)-piperidine, particularly in the critical temperature of dissolution in hexane, and which are used in a mixture, forming a number of compounds with gradually varying characteristics. Owing to this, a greater homogeneity of the fluorocarbon phase is achievable in the emulsions and it becomes possible to enhance the stability of the emulsion particles stabilized by an ethylene oxide-propylene oxide block copolymer, with the absence of toxicity for large animals. A mixture of TPFCAs is prepared by electrochemical fluorination of n-piperidinoheptafluorotoluene in anhydrous hydrogen fluoride. The use of this mixture of TPFCAs instead of individual perfluoro-N-(4-methylcyclohexyl) piperidine simplifies, speeds up the process for preparing perfluorinated organic compounds, makes it cheaper, and provides conditions for broader application of gas transport emulsions based thereon.
CN101590098A Medicine for treating scalds and burns The invention relates to a medicine for treating scalds and burns, which can alleviate pain, has high recovery speed and remains no scar. The technical scheme is that: the medicine is characterized in that the medicine comprises the following components by weight: 94 to 95% of soybean oil, 1 to 2% of mercurous chloride, 2 to 3% of borneol and 1 to 2% of beeswax.
WO2013030177A1 Abuse resistant tablet comprising oxycodone and paracetamol The invention relates to a tablet formulation based on paracetamoland oxycodone. The invention also relates to a process for preparing said tablet and to the use thereof.
CN1746164A Protein antagonist with water channel A water-channel protein antagonist is that R1 is choosed from hydrogen, SO2NH2, C1-C4 straight chain or branched chain alkyl, R2 is choosed from phenyl, one or above halogen substituted phenyl, and X is O or S independently.
WO2009152724A1 Use of paederosidic acid methyl ester in manufacture of medicaments for treating pain and/or inflammation. Use of paederoside acid methyl ester in manufacture of medicaments for treating pain and inflammation. There is a good effect of paederoside acid methyl ester on treating central pain, peripheral pain and inflammation. Therefore, medicaments can be formulated by using paederoside acid methyl ester, alone or combined with other pharmaceutically acceptable components,for treating pain and/or inflammation.
CN102106972B Medicament for treating empyrosis and scalding and acute skin bruise and contusion, preparation method and detection method The invention relates to a Chinese and western medicinal compound preparation for treating empyrosis and scalding and acute skin bruise and contusion, a preparation method and a detection method. The Chinese and western medicinal compound preparation is prepared from chlorhexidine acetate, borneol, common bletilla pseudobulb, sanguisorba root and rhubarb, and can be formed into a film coating agent and the like. A quality control method comprises the following steps of: identifying rhubarb, borneol, sanguisorba root and chlorhexidine acetate; performing a film coating experiment and the test of the pH value and relative density; and measuring the content of rhubarb and the content of sanguisorba root. The Chinese and western medicinal compound preparation has the characteristics of definite curative effect, fewer side effects and convenience for quality control.
WO2010100199A1 Fluconazole carboxylic ester derivatives, synthesis, and use in long acting formulations This invention relates to compounds represented by the structural formula (1) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein: R' is a saturated or ethylenically unsaturated linear or branched alkylene group having from 2 to 4 carbon atoms or a saturated or ethylenically unsaturated cycloalkylene group having from 4 to 8 carbon atoms, and OY is a sterol residue. These compounds are useful pharmaceutical agents with improved solubility and bioavailability characteristics.
US20110130452 Store-operated calcium cellular assay The present technology provides a cell based assay for identifying compounds that modulate store-operated ionic calcium levels using itpr mutant cell lines, such as itpr-ku cells, which have abnormal ionic calcium levels.
US20110165064 Methods and compositions related to clot-binding compounds Disclosed are compositions and methods related to clot-binding compounds. For example, disclosed are compositions comprising a surface molecule and at least one modified clot-binding compound. The modified clot-binding compound can selectively bind to clotted plasma protein, wherein the composition causes clotting and amplifies the accumulation of the composition in tumors. The modified clot-binding compound can enhance the clotting in tumors compared to its unmodified derivative. The disclosed targeting is useful for treatment of cancer and other diseases and disorders.
EP1545500A1 Paclitaxel composition for the intravesical treatment of bladder tumor and preparation method thereof The present invention relates to a paclitaxel composition and the preparation methods thereof for the treatment of bladder cancer wherein said paclitaxel composition comprises 4~90% by weight of at least one selected from the monoglycerides, 0.01~90% by weight of at least one oil, 0.01~90% by weight of at least one emulsifier and 0.01~20% by weight of paclitaxel. The composition of the present invention can treat bladder cancer effectively since the composition solubilizes paclitaxel, does not form aggregates, adsorbs well on the bladder wall and penetrates into the muscle layer of the bladder.
US20080207715 Novel Inhibitors of Glutaminyl Cyclase The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein: R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, -alkoxy, -thioalkyl, —C(O)O-alkyl and —C(O)OH; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)O-alkyl and —C(O)OH; alkenyl; alkynyl; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; -aryl-aryl; -aryl (monocyclic or bicyclic); heteroaryl (monocyclic or bicyclic); heterocyclyl; or R2 together with R4 may form a carbocyclyl group optionally substituted by one or more alkyl groups; R3 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, amino, halogen, haloalkyl, hydroxyl, -alkoxy, -thioalkyl, —C(O)OH and —C(O)O-alkyl; alkenyl; -alkyl-aryl; -alkyl(aryl)2, -alkyl(heteroaryl)2, -alkyl(aryl)(heteroaryl), -alkyl-heteroaryl; -alkyl-heterocyclyl which heterocyclyl group may optionally be substituted by one or more groups selected from alkyl, hydroxy and oxo ; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-aryl; -aryl-O-aryl, -heteroaryl-heteroaryl; -aryl; heteroaryl; heterocyclyl; -aryl-alkyl-aryl; -aryl-O-alkyl-aryl; -alkyl-C(O)—NH-alkyl-aryl; -alkyl-C(O)—NH-alkyl-heteroaryl; -alkyl-C(O)—NH-alkyl-heterocyclyl; -alkyl-C(O)—(N-piperidinyl) or -alkyl-C(O)—(N-pyrrolidinyl) in which piperidinyl or pyrrolidinyl may optionally be fused to optionally substituted phenyl. R4 represents H or alkyl.
WO2007108754A1 Crystalline forms of n- {2-tert -butyl -1- [ (4,4- dif luorocyclohexyl) methyl] -lh-benzimidazol-5- yl}ethanesulfonamide salts A salt of the compound N-{2-tert-butyl-1-[(4,4-difluorocyclohexyl)methyl]-1H-benzimidazol-5-yl}ethanesulfonamide, which is an ethanesulphonic acid salt, a sulphuric acid salt, an ethane disulphonic acid salt, a hydrochloric acid salt, a hydrobromic acid salt, a phosphoric acid salt, an acetic acid salt, a fumaric acid salt, a maleic acid salt, a tartaric acid salt, a citric acid salt, a methanesulphonic acid salt, or a p-toluenesulphonic acid salt of said compound.
US20080227777 Pyrazolopyridine derivatives as inhibitors of beta-Adrenergic Receptor Kinase 1 The invention relates to 6-amido substituted pyrazolopyridine derivatives of the formula (I) useful as inhibitors of beta-adrenergic receptor kinase 1 (βARK-1), compositions containing such compounds and their use for the treatment and prevention of chronic heart failure, hypertension, myocardial ischemia and hepatitis C virus (HCV) infections, and for the prevention of opiate addiction.
CN101732345A Cisplatin spinal tumor slow-release implant and preparation method thereof The invention belongs to the field of pharmacy, and relates to a controlled-release medicinal preparation, in particular to a cisplatin spinal tumor slow-release implant which takes polylactic acid-glycolic acid copolymer (PLGA) as a carrier and cisplatin as a main medicament for treating the spinal tumor and a preparation method thereof. The weight ratio of the cisplatin to the PLGA is 1:99-40:60. A cisplatin slow-release micro-ball is prepared through reemulsifying-solvent volatilization method, and the micro-ball is tabletted to obtain the cisplatin slow-release implant for interstitial chemotherapty after the spinal tumor and the other tumor surgeries. Experiments prove that: the cumulative medicament release rate of the cisplatin slow-release implant after 38 days can reach 84 percent, the sustained release time in the body can reach 36 days, the local medicament concentration is high and an effect of inhibiting the tumor is obvious.
CN102971424A High-affinity nucleic acid aptamers against sclerostin protein Described are nucleic acid aptamers that are able to bind to and inhibit the function of sclerostin, which is an important negative regulator of bone growth. The aptamers have application as therapeutics for diseases of bone including osteoporosis, osteopenia, osteoarthritis and other osteoporosis-related conditions and complications.
CN102423299A Preparation method for novel drug-loaded chitosan nano-microspheres The present invention discloses a method for preparing drug-loaded chitosan nano-microspheres, wherein sorbitan sesquioleate is adopted as an emulsifying agent, vanillin is adopted as a cross-linking agent, and an emulsifying and cross-linking method is adopted. The method comprises: dissolving a certain amount of chitosan and a certain amount of 5-fluorouracil in a certain amount of an acetic acid solution with a mass fraction of 1%; after completely dissolving, slowly adding the resulting solution to a certain amount of a liquid paraffin oil phase, and rapidly stirring at a room temperature to form a white emulsus water-in-oil emulsion, wherein the resulting solution is adopted as the water phase, the liquid paraffin oil phase contains a certain amount of an emulsifying agent; adding a certain amount of a cross-linking agent solution to the reaction system, and continuously stirring for a certain time; carrying out centrifugal separation, collecting the prepared drug-loaded nano-microspheres, completely washing respectively by petroleum ether and acetone, carrying out freeze drying to obtain the yellowish drug-loaded chitosan nano-microsphere powder, wherein the particle size of the prepared drug-loaded chitosan nano-microspheres is 100-150 nm, the sphericity is good, the controlled release effect is good, the encapsulation efficiency is 90-96%, the drug loading rate is 20-25%, and the drug-loaded chitosan nano-microspheres can meet clinical oral requirements and injection requirements. In addition, the method has a simple process, and is applicable for the large-scale production.
CN1883481A Composition of leukotrienes antagonist oral liquid The invention relates to an oral liquid of leukotriene antagonist against allergy, inflammation, asthma that can be used as cell protecting agent, comprising at least a buffer solution and Montelukast dissolved in the buffer solution and its pharmaceutically acceptable salts. The pH of the buffer solution is between 7-11, and the buffer solution includes at least water, pharmaceutically acceptable alcohols, buffering agents and pharmaceutically acceptable additives.
US20070265289 2-Aminopyrimidine Derivative The invention relates to a compound useful as remedies or preventives for IKK2-related inflammatory diseases or autoimmune diseases, or that is, a 2-aminopyrimidine derivative having a 2-hydroxyphenyl group at the 6-position thereof and having a saturated cyclic group that contains one nitrogen atom, such as piperidine, at the 4-position thereof. The pharmaceutical composition of the invention and the compound of the invention have an excellent antiinflammatory effect based on the IKK2-inhibitory effect thereof, and are therefore useful for remedies and preventives for inflammatory diseases and autoimmune diseases, especially for rheumatoid arthritis.
WO2007050576A3 A method of preparing a 4-oxo-1- (3 substituted phenyl) -1, 4-dihydro-1, 8-naphthyridine-3- carboxamide phosphodiesterase-4 inhibitor The invention is directed tc methods of preparing a compound of the structural formula (22) crystal form of structural formulae (21) and its free acid.
CN103083224A Method for preparing dexamethasone slow-release medicine carrier The invention relates to a method for preparing a dexamethasone slow-release medicine carrier. The method comprises the following steps of: (1) adding silk fibroin and polyethylene oxide (PEO) into water, and dissolving to obtain a solution a; (2) dissolving dexamethasone into tween-80, adding to vegetable oil, and mixing to obtain a solution b; and (3) mixing the solution a and the solution b in a volume ratio of (50-100): 1, stirring, performing electrostatic spinning and alcohol fumigation cross linking, and thus obtaining the dexamethasone slow-release medicine carrier. A silk fibroin/ PEO composite nano fiber carrying the dexamethasone and having a shell-core structure is prepared by using the electrostatic spinning technology for the first time, is used as a new slow-release medicine carrier, and achieves a long slow-release effect; and the silk fibroin and the PEO used in the method have good biocompatibility, are green and safe, and have already been widely applied in the field of biomedicine.
CN101804040A Ketoprofen slow-release orally disintegrating tablets The invention relates to ketoprofen slow-release orally disintegrating tablets serving as a non-steroidal anti-inflammatory medicament and a preparation method thereof. The method mainly comprises the following steps of: preparing ketoprofen slow-release fine particles by a spray drying method; and preparing the fine particles into the orally disintegrating tablets by a direct powder tabletting method. The orally disintegrating tablets have the characteristics that: the orally disintegrating tablets are convenient to take; the orally disintegrating tablets can quickly disintegrate, slowly release the fine particles and be swallowed after being wetted by spittle without drinking water; the orally disintegrating tablets are particularly suitable for old persons, children and special patients having difficulty in swallowing such as patients with coma; the medicament can be slowly released in the body, and overcomes the defects that the conventional ketoprofen has short half-life period and needs to be frequently taken; and the orally disintegrating tablets have simple preparation process and easy industrial production.
WO2007007625A1 Pharmaceutical for prevention of hypersensitivity Disclosed is a pharmaceutical composition for preventing hypersensitivity induced by taxoid. A pharmaceutical composition for preventing hypersensitivity induced by taxoid, the composition comprising a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: (I) wherein R1: a substituted phenyl; R2: a halo-substituted phenyl; G: >C-OH or >S→O; and n:1 or 2.
WO2008024299A2 Combination with bis(thiohydrazide amides) for treating cancer Disclosed herein are methods of treating an immunosensitive cancer with bis(thio-hydrazide amides) or pharmaceutically -acceptable salts thereof and an immunotherapy.
US20080280934 Porphyrin ring compound containing cyanovinyl group; reacted with Vilsmeier reagent,complexed with metal ion in prsence of an acid and oxidizer; skin disorders; antiinflammatory agents; anticancer agents; antitumor agents; vascular disorders, vision defects, urogenital system disorders; immunology Method of preparing a porphyrin derivative starting from a meso-substituted porphyrin compound. According to the invention, the meso-substituted porphyrin compound used is a meso-(2′-cyanovinyl)-substituted porphyrin compound, wherein said meso-(2′-cyanovinyl)-substituted porphyrin compound, in a form in which its porphyrin ring is complexed with a bivalent metal ion is converted, in the present of an acid for which 0, R<2>, R<3> and X are defined as in a specification. The invention also relates to a preparation method of the compounds, medical compositions containing the compounds and the application of the compounds in preparing medicines for curing and/or preventing infectious diseases.
EP2398324A1 PYRAZOLO [4,3-c]CINNOLIN-3-ONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS The present invention is directed to pyrazolo [4,3-c] cinnolin-3-one compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
US20120022126 Method Of Treating Diabetes Mellitus The invention provides methods of treating a diabetic subject comprising administering a glucosylceramide synthase inhibitor to the subject.
CN1679523A Analgesic injecting powder preparation and preparation thereof An analgesic powder injection is prepared from tramadol hydrochloride through freeze drying. Its advantages are high activity and high stability.
WO2011010364A1 Compound having neurite-outgrowing activity Disclosed is a novel compound having a neurite-outgrowing activity and is therefore useful for the prevention or treatment of neurodegenerative diseases. Specifically disclosed is a compound represented by formula (I) [wherein X represents OR or NR1R2; Y represents OH, NR3R4, -NHC(=NH)NHR5 or –NHC(=NH)R5; and Z represents a hydrogen atom, a linear or branched alkyl group having 1 to 5 carbon atoms, or a 5- to 6-membered aryl group which may have one or two atoms independently selected from a nitrogen atom, a sulfur atom and an oxygen atom] or a pharmaceutically or veterinarily acceptable salt thereof.
CN101040995A Valid target of garlic oil and the application in preparing many kinds of medicine The invention relates to an effective part of Chinese drug and relative application, wherein, the effective part is a compound whose main components are allyl disulfide (DADS) and methacrylic trisulfide (MATS), without diallyl trisulfide (DATS) as allicin, while the effective part is significant different from garlic oil in quality and quantity, which is separated and extracted from garlic oil. The effective part has the functions as antibiosis and antiviral (as anti-AIDS and anti-herpesvirus) outside the body, and the anti-tumor function (as anti-leukemia), and anti-thrombus) function. Compared with allicin, the invention has high stability and low side effect, while the effective part can be used to prepare the drug for treating virus, bacterial, tumor and thrombus, with wide clinic application.
WO2008063116A1 Indozalyl sulphonamide derivatives useful as glucocorticoid modulators Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
CN103127143A Inhalation drug composition with budesonide and nitric oxide synthase (NOS) inhibitor An inhalation drug composition with budesonide and a nitric oxide synthase (NOS) inhibitor comprises the budesonide which serves as an active ingredient, an amino acid derivative which serves as the NOS inhibitor, and one or more types of drug auxiliary materials applicable to inhalation.
US8012496 Gastric retention controlled drug delivery system The present invention provides a gastric retention controlled drug delivery system comprising: (a) a controlled release core comprising a drug, a highly swellable polymer and a gas generating agent, said core being capable of swelling and achieving floatation rapidly while maintaining its physical integrity in gastrointestinal fluids for prolonged periods, and (b) a rapidly releasing coat composition comprising the same drug as in the core and pharmaceutically acceptable excipients, wherein the coating composition surrounds the core such that the system provides a biphasic release of the drug in gastrointestinal fluids.
US20100222334 Pharmaceutical Formulation of Valsartan The present invention relates to a pharmaceutical composition in a form of suspension for oral administration comprising valsartan or its pharmaceutically acceptable salts and at least one or two or more of the components selected from glycerol or syrup or the mixture thereof, a preservative, a buffer system and a suspending/stabilizing agent. The present invention further relates to the therapeutic uses of the pharmaceutical composition.
WO2007146547A3 Piperazine enamines as antiviral agents This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and azaindole piperazine enamine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.
US6887864 Anticancer agents, a benzoylamino-azepan-3-yl-isonicotinamide compounds This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.
US7683080 purification from sulfide/sulfone derivatives; crystallization; proton pump inhibitors The present invention provides a stable 2-(2-pyridylmethyl) sulfinyl-1H-benzimidazole (lansoprazole) comprising either greater than 500 ppm and not more than about 3,000 ppm water or greater than 200 ppm and not more than about 5,000 ppm alcohol, or both. The present invention provides a method of preparing a stable lansoprozole as well as a pharmaceutical composition containing same. The present invention further provides a method of purifying lansoprazole that is substantially free of sulfone and sulfide derivatives.
EP1423362B1 New mandelic acid derivative and its use as thrombin inhibitor There is provided a compound of formula (I) and pharmaceutically-acceptable derivatives (including prodrugs) thereof, which compound and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
US20070173534 Pyridinic sulfonamide derivatives method of production and use thereof New pyridinic sulfonamide derivatives represented by a general formula (I), wherein R1 represents a mono- or polyhalogenated C1-12-alkyl or a mono- or polyhalogenated C3-8-cycloalkyl group. The method of production of such derivatives and their use as active therapeutic substance in the treatment of diseases such as inflammation, arthrosis, cancer, angiogenesis and asthma are also reported.
CN101181601B Externally used detumescence ding-tong wine for curing orthopaedics illness The present invention relates to an external detumescence and pain released wine for curing orthopedics disease. The invention is characterized in that the prescription consists of the following raw medicines by weight: 5 to 35 parts of dragon's blood, 15 to 35 parts of frankincense, 15 to 35 parts of myrrh,15 to 35 parts of safflower,15 to 35 parts of fresh szechuan lovage rhizome, 20 to 40 parts of common burreed rhizome, 15 to 35 parts of rhizoma zedoariae, 15 to 35 parts of angelica tail, 20 to 30 parts of fresh rhubarb, 20 to 40 parts of fresh pinellia tuber, 20 to 40 parts of fresh rhizoma arisaematis, 20 to 40 parts of nux vomica, 15 to 35 parts of amphor, 10 to 25 parts of manchurian wildginger, 30 to 40 parts of ephedra herb, 20 to 30 parts of fresh common monkshood mother root, 20 to 30parts of fresh kusnezoff monkshood root, 30 to 45 parts of paniculate swallowwort root and 4000 to 5000 parts of alcohol with a concentration of 55 percent. The external detumescence and pain released wine for curing orthopedics disease provided by the present invention has the advantages that the external detumescence and pain released wine for curing orthopedics disease has functions of promoting blood circulation, removing blood stasis, and relieving swelling and pain for obvious partial hematoma due to bones and muscles injury; and the invention is also used for curing diseases such as closed fracture, dislocation of joint, soft tissue injury, hypostasis and detumescence and pain. Besides, the invention also has the advantages of short treatment period, quick effect, low price and wide application, with a total effective rate of more than 90 percent.
CN102836160A Combined medicament for treating cancers The invention relates to a combined medicament for treating cancers. The combined medicament consists of sorafenib and ABT-263 in the molar ratio of (0.75-15):1, and has a good effect. As proved by in-vivo and in-vitro experimental study, apoptosis of cancer cells can be induced effectively by applying sorafenib and ABT-263 together, a remarkable curative effect on cancer treatment is achieved, an achieved anti-cancer effect has a synergic function, and the combined medicament is an efficient low-toxicity anticancer medicament.
EP2188297B1 Pyrrolo [2,1-c][1, 4] benzodiazepine-glycoside prodrugs useful as a selective anti tumor agent The present invention provides novel pyrrolo[2,1-c][1, 4]benzodiazepine- glycoside prodrug of general formula (1a-b), useful as selective anticancer agents. The present invention also provides a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine-glycoside prodrugs of general formula (1a-b). This invention also provides activation of these produgs by E.coli β galactosidase and envisaged that these molecules are toxic to human cancer cell lines in the presence of the enzyme E.coli β -galactosidase. The prodrugs (1a and 1b) were also found to be toxic to human cancer HepG2 cells even in the absence of the E.coli β-galactosidase. The toxic effect of the molecules when activated was similar to that of the parent molecules (6a and 6b), respectively.
CN102702116A 4-(3-chloro-4-methoxylanilino)-6-(3-amidophenyl)quinazoline compound or pharmaceutically-acceptable salt thereof and preparation methods and applications thereof The invention discloses a 4-(3-chloro-4-methoxylanilino)-6-(3-amidophenyl)quinazoline compound shown as a structure formula (I). In the structure formula (I), R is any one of -H, -COCH3, -COCF3, -COCH=CHCOOH, -COCH2Cl, -COCCl3, -COCH=CH2, -COC(CH3)3, -COCH2CH3 and -COHBrCH3. The invention further relates to a preparation method of the compound, a pharmaceutically-acceptable salt of the compound, and applications of the compound and the pharmaceutically-acceptable salt thereof to preparation of an antitumor medicament.
EP1536795A1 Inverse agonists acting at virus-encoded g protein-coupled receptors The present invention relates to a group of non-peptidergic compounds which compounds are inverse agonists acting on the Human cytomegalovirus (HCMV) encoded US28 receptor. In addition, the invention relates to the use of these compounds in the manufacture of a medicament having inverse agonist activity on HCMV encoded US28 receptor. Further, the invention relates to the use of these compounds in the manufacture of a medicament for inhibiting viral infections, and particularly in the treatment of HIV infections, such as in AIDS.
US20080293618 Cyclopropyl-fused pyrrolidine derivatives as dipeptidyl peptidase iv inhibitors The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.
US20100209519 Pharmaceutical composition for inhalation delivery and fabrication method thereof A pharmaceutical composition for inhalation delivery is provided, including drugs and a gelatin nanoparticle encapsulating the drugs to form a drug-gelatin nanocomplex, wherein the surface of the gelatin nanoparticle is modified with cell-targeting molecules. A method for fabricating the pharmaceutical composition for inhalation delivery is also provided.
CN101766578B Tablet containing Rosuvastatin calcium and preparation process thereof The invention belongs to the filed of medicine, in particular to a tablet containing Rosuvastatin calcium and a preparation process thereof. As for the tablet containing the Rosuvastatin calcium of the invention, lactose and hydroxypropyl cyclodextrin with the ratio ranging from 1:1 to 2.5:1 are selected to serve as fillers, and opacifier medicinal iron oxide red is added in production process. In the invention, a direct powder tabletting method is utilized for taletting, and the prepared tablet containing the Rosuvastatin calcium has the characteristics of stable long-term preservation, rapid disintegration rate, high dissolution and high bioavailability.
CN101074254A Sequence against human esophagus cancer invasion and transfer A sequence against human-body esophagus cancer invasion transfer, its plasmid and usage in preparation of medicine against human-body esophagus cancer invasion transfer are disclosed. The sequence is SEQ ID NO: 1 or SEQ ID NO: 2, the plasmid is pGCsi/U6/neo/GFP/cyclin B1-1 and pGCsi/U6/neo/GFP/cyclin B1-2.
US20120015941 Antibacterial Amide and Sulfonamide Substituted Heterocyclic Urea Compounds The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.
WO2012164927A1 Hair growth and hair restoration material Provided is a novel hair growth and hair restoration material having excellent efficacy in hair growth and hair restoration for both men and women, even when the components thereof are at ultra-dilute concentrations; the hair growth and hair restoration material being characterized in containing a steryl glucopyranoside, preferably a cholesteryl glucopyranoside, represented by general formula (I). (In the formula, Z represents a sterol residue from which the hydroxyl group attached to the 3-position of a cyclopentanohydrophenanthrene ring has been removed.)
CN103006647A Use of 3-amido-2-pyridone derivative The invention relates to the field of pharmaceutical chemistry, in particular relates to a medical use of a 3-amido-2-pyridone compound, and a pharmaceutical composition containing such a compound, and especially an application as a cholinesterase inhibitor. Pharmacological experiments show such a compound has good cholinesterase inhibition activity, and has favorable application prospects in the field of treating Alzheimer disease, schizophrenia, chronic brain damage, facial paralysis, hemiplegia and the like.
US20100227812 Method of supplementing the diet and ameliorating oxidative stress A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of an active compound having the chemical structure: where n=1-4 and X is selected from the group consisting of hydrogen, lithium sodium, potassium, rubidium, cesium and francium.
US20120076776 Method for treating inflamation by lymphocyte depletion or sequestering A method for preventing inflammation, comprising administering to a subject a lymphocyte sequestrating or depletion agent before the onset of inflammation. A method for treating inflammation caused by an injury or an infection, comprising depleting immune lymphocyte of a subject by administering to said subject a lymphocyte sequestrating or depletion agent during or after said event. A method for preventing or treating abdominal adhesion comprising administering to a subject a lymphocyte sequestering or a lymphocyte depletion agent.
US7625710 Methods for determining 2F1-binding compounds 2F1 polypeptides are provided, along with DNA sequences, expression vectors and transformed host cells useful in producing the polypeptides. Soluble 2F1 polypeptides find use in inhibiting prostaglandin synthesis and treating inflammation.
CN101530411A Application for taking NO donor-type compounds as P-glycoprotein inhibitors and tumor multi-drug resistance reversal agents The invention relates to the medical field of sensitizing antitumor medicaments and reversing tumor multi-drug resistance, in particular to inhibiting effect of nitric oxide (NO) donor-type alkoxy biphenyl carboxylic acid compounds on P-glycoprotein, and application thereof in reversing tumor multi-drug resistance. The characteristics of the invention are summarized as follows: NO donor-type alkoxy biphenyl compounds are characterized in that the compounds have alkoxy biphenyl carboxylic acid parent framework and furazan nitrogen oxide type NO donor radicals, are formed by connected amino acids unequal in length with radicals, can be taken as P-gp inhibitors and tumor multi-drug resistance reversal agents, can remarkably increase the cell uptake amount of P-gp substrates, reduce substrate efflux, regulate the expression of P-gp down, can be used in combination with the antitumor medicaments to increase the concentration of the compounds in multi-drug resistance tumor cells, have a drug-resistance reversal multiple up to hundreds of times, enable multi-drug resistance cell strains to recover sensibility to chemotherapeutic medicaments, and have extensive application prospects.
US7294630 Piperazinyl piperidine tachykinin antagonists The present invention provides compounds of formula (I): wherein each R independently represents a halogen atom or a C1-4 alkyl group; R1 represents a C1-4 alkyl group; R2 represents hydrogen or a C1-4 alkyl group; R3 represents hydrogen or C1-4 alkyl group; R4 represents a trifluoromethyl group; R5 represents hydrogen, a C1-4 alkyl group or C(O)R6; R6 represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; or a pharmaceutically acceptable salt or solvate thereof; compositions containing the same, processes for their preparation and methods for their use in the treatment of conditions mediated by tachykinins.
US20110152168 Antiadhesive carbohydrates Provided is a pharmaceutical or dietetic product, which serves for reducing and/or blocking the adhesion of pathogenic substances and organisms to eucaryontic cells, in particular mammal cells. Said preparation contains at least one carbohydrate having an uronic acid unit on one of the ends thereof. 10 to 100% of the present, terminal uronic acid units pertaining to the carbohydrates are provided with a double bond that is especially situated between the C4 and C5 atom.
EP0859840B1 Biologically active eph family ligands A novel ligand (Efl-6) that binds the Elk subfamily of Eph receptors is identified, and methods for making the soluble Elf-6 ligand in biologically active form is described. A cDNA clone encoding this novel protein enables production of the recombinant protein, which is useful to support neuronal and other Eph receptor-bearing cell populations.
WO2006025251A1 Physiologically active substances biselide a, biselide b, and biselide c, processes for producing these, and uses of these [PROBLEMS] A novel anticancer agent which is effective against multiple-drug-resistant cancer cells. [MEANS FOR SOLVING PROBLEMS] Physiologically active substance biselide C, which is represented by the following formula (I): or a pharmacologically acceptable salt thereof.
WO2004031174A8 Imidazol-1-ylmethyl pyridazine derivatives The invention provides imidazol-l-ylmethyl pyridazine derivatives of the Formula (I), that bind to GABAA receptors. In the above formula, R1, R2 R3, R4, R5, R6 and Ar are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
WO2013144860A1 A therapeutic agent for treatment of blood vessels A therapeutic agent for the treatment of blood vessels, preferably applied to coronary stents, characterised in that it comprises compounds with a 2,3-diphenyl-4H- pyrido[1,2-a]pyrimidine-4-one nucleus.
WO2012105715A1 Novel external preparation The present invention provides an adhesive preparation comprising (3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione (hereinafter to be referred to as "compound 1"), which suppresses metabolites production and is superior in skin permeability. The adhesive preparation of the present invention containing a support and an adhesive layer formed on one surface of the support, wherein the adhesive layer comprises (i) compound 1 or a physiologically acceptable acid addition salt thereof, (ii) an adhesive, and (iii) an additive comprising a particular skin permeation enhancer, can remarkably enhance the skin permeability of compound 1.
WO2007085202A1 Oxamic acid derivatives,preparation methods and medical uses thereof Compounds represented by the general formula I, their pharmaceutically acceptable salts, solvates are disclosed. The definitions of substituents of formula I are the same as description. The pharmaceutical compositions containing the compounds of general formula I, their preparation methods and their uses in manufactures of pharmaceutical medicaments for treatment or preventing various diseases and dangerous factors relating to human being’s peroxisome proliferator-activating receptor (hPPAR).
US20110091556 Antimicrobial compositions and methods of use The present invention relates to compositions and methods for decreasing the infectivity, morbidity, and rate of mortality associated with a variety of pathogenic organisms and viruses. The present invention also relates to methods and compositions for decontaminating areas colonized or otherwise infected by pathogenic organisms and viruses. Moreover, the present invention relates to methods and compositions for decreasing the infectivity of pathogenic organisms in foodstuffs. In particular, decreased pathogenic organism infectivity, morbidity, and mortality is accomplished by contacting the pathogenic organism with an oil-in-water nanoemulsion comprising an oil, an organic solvent, and a surfactant dispersed in an aqueous phase.
CN103463076A Application of Lycojaponicumin C in respiratory syncytial virus resistant medicine The invention discloses an application of Lycojaponicumin C in preparation of a respiratory syncytial virus resistant medicine. Experiments show that the Lycojaponicumin C has a remarkable inhibitory effect on respiratory syncytial virus (RSV). The invention provides experimental basis for clinical application of Lycojaponicumin C for treating diseases caused by RSV infection, has certain guiding significance in development of respiratory syncytial virus resistant medicine, and has important reference value.
CN101953842B Application of syringin in preparation of medicine for treating acute gout The invention provides a new application of syringin in medical science, in particular to application of syringin in the preparation of a medicine for treating acute gout. Syringin is extracted and separated from acanthopanax roots and other plants, and the extraction method comprises the following steps of: refluxing and extracting dry acanthopanax root powder with ethanol, recovering the ethanol, adding water to the concentrated solution, stirring to obtain a mixed suspension, extracting with petroleum ether, extracting the water layer with acetic ether, merging the acetic ether layer, concentrating under reduced pressure to obtain an extract, separating by using a silica gel column, carrying out gradient elution by using chloroform and methanol in sequence to obtain a coarse crystal, and recrystallizing with methanol to obtain a syringin crystal. Experimental researches show that syringin can protect an acute gout model due to human vascuoar endothelial cell damages caused by urateand inhibit the expression of ICAM-1 (Intercellular Adhesion Molecule-1); thus, syringin can be used for preparing a medicine for treating acute gout.
EP2459550A2 R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and l-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial Disclosed herein are R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial. Because the R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt is more soluble and less toxic and has less side effects as an antimicrobial agent than hydrochloride and the other salts (D-aspartate and phosphate) conventionally used, the salt may be useful for oral and injectable administration.
CN103316043A Medical application of composition comprising carbon material and active particles The invention provides an application of a composition used for preparing medicines used for treating or preventing Helicobacter pylori infection. The composition comprises a carbon material and active particles which is loaded on the carbon material and whose material is silver, gold, aluminum, zinc, copper or titanium dioxide.
US20100286218 Liquid preservative compositions A liquid preservative composition comprises (a) an alkanol fatty monoester; and (b) an aqueous isothiazolinone solution, an alkanol-substituted aromatic compound, or a combination thereof; and is free from formaldehyde, formaldehyde-releasing compounds, and paraben compounds. Preferred compositions comprise glyceryl caprylate, together with either phenethyl alcohol or an aqueous 2-methyl-4-isothiazolin-3-one solution.
EP2420496A2 Antiepileptic, hypocholesterolemic and neuroprotective compound The present invention describes a compound of formula (I) its hydroxy acid form, the pharmaceutically acceptable salts of said hydroxy acid and pharmaceutically acceptable prodrugs and solvates of the compound and of its hydroxy acid form and, in particular, said compound, its hydroxy acid form, salts, etc. for its use in the prevention of: neurodegenerative diseases, cognitive deterioration, diseases associated with undesired oxidation, age-associated pathological processes and progeria, epilepsy, epileptic seizures and convulsions, cardiovascular diseases such as atherosclerosis, atrial fibrillation, dyslipemia, hypercholesterolemia, hyperlipidemia, and hypertriglyceridemia, or fungal or viral infections.
EP2640469A1 Signal transduction pathway modulation Provided herein are methods and compositions for modulating signal transduction pathways by regulating the expression and/or activity of Midline-1, enabling the inhibition of airways inflammation, the inhibition of airways hyperresponsiveness, the inhibition of rhinovirus-associated inflammation, and reductions in cytokine and chemokine release. Methods and compositions disclosed herein facilitate the treatment and prevention of conditions associated with airway inflammation, airway tissue remodelling and rhinovirus-associated inflammation and symptoms, manifestations and exacerbations thereof, in particular of allergic diseases such as allergic airways diseases including asthma.
US20080187513 Treatment of Solid Cancers The present invention relates generally to the field of cancer including tumor therapy. More particularly, the present invention relates to the treatment of solid cancers, including solid tumors, and the prevention or reduction of cancer metastasis, by chemoablation of cancer cells by an agent which also stimulates the generation of cancer-specific T-cells, a process referred to herein as immunostimulatory chemoablation. The present invention further contemplates combination therapy comprising immunostimulatory chemoablation and one or more other therapeutic regimens, which enhance, co-operate and/or synergize with the cancer-specific T-cells induced by the chemoablation. The present invention also relates to pharmaceutical compositions for use in treating cancers.
US20080269330 Nutrition Containing Fat Blend The invention relates to the use of long chain polyunsaturated fatty acids for the manufacture of a nutritional composition for feeding infants of a mother who suffered from a metabolic disorder during pregnancy and to a corresponding composition. Said composition comprises a n-3 polyunsaturated fatty acid fraction containing at least 0.1 wt docosahexaenoic acid (DHA) based on total weight of the lipid, at least 0.01 wt % n-3 docosapentaenoic acid (DPAn-3) based on total weight of the lipid, and at least 0.01 wt. % eicosapentaenoic acid (EPA) based on total weight of the lipid, wherein the sum of DHA, DPAn-3 and EPA is below 1 wt. % of total lipid.
US20100278757 Water-Absorbent Adhesive Compositions and Associated Methods of Manufacture and Use An adhesive composition is provided that is water-insoluble yet water-absorbent, i.e., capable of absorbing up to 15 wt. % water or more. The composition is composed of a film-forming hydrophilic polymer with at least one linear segment having a plurality of recurring polar groups along the polymer backbone, a complementary multifunctional polymer with a plurality of recurring functional groups that noncovalently bind to the polar groups on the film-forming polymer, and a plasticizer. A method for manufacturing the adhesive composition is provided as well.
CN103432209A Preparation method of rhizoma corydalis crude drug The invention discloses a preparation method of rhizoma corydalis medicinal slices, which comprises the following steps: taking rhizoma corydalis used as the technical material, removing impurities, cleaning, moistening, cutting into slices, microwave drying, processing with vinegar, processing with Chinese angelica juice, and drying so as to obtain the rhizoma corydalis medicinal slices. The medical stone is added into rhizoma corydalis processed with vinegar and fried with the rhizoma corydalis, the porous structure of the medical stone can plays a role in absorbing heavy metal ions in medicinal materials, beneficial metal ions are supplemented, and processing the mixture with Chinese angelica juice after stir-frying, so that the effects of replenishing blood, activating blood, regulating menstruation, relieving pain, nourishing blood and nourishing liver are added.
US20120028973 Nitroimidazooxazines and their uses in anti-tubercular therapy The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
CN101006996A A drug for treating calculus in urinary system and hyperuricemia and its preparation method The invention disclosed a kind of drug for treating calculus of urinary system and hyperuricacidemia, the preparative method is also mentioned in the invention. The main materials of the invention are potassium citrate, sodium citrate and citric acid. After mixing the main materials with some pigment, essence as well as other additives according to appropriate portion, stirring, drying, weighting and packing to get the granule drugs. The invention has a special formula and preparing method as well as notable treating effects. The drug in the invention can also coordinate ESWL, improve the stone removing effect and promote the dissolving and discharging of the remained stone.
CN102050814A Ester derivatives of dabigatran The invention relates to ester derivatives of dabigatran shown in the formula I and non-toxic pharmaceutically acceptable salts thereof, a medical composition containing the ester derivatives and the non-toxic pharmaceutically acceptable salts as active components, and application of the ester derivatives and the non-toxic pharmaceutically acceptable salts as well as the medical composition, wherein R1 represents H or alkyl of C1-C5; R2 represents H or alkyl of C1-C3; and R3 represents alkyl of C1-C8 or substituted alkyl.
US20100247688 Pirenzepine and derivatives thereof as anti-amyloid agents The present invention relates to a compound that is capable of inhibiting the formation of β-amyloid plaques, of reducing and/or retarding the increase the β-amyloid plaque load in the brain of an animal, particularly a mammal, but especially a human. In particular, the invention relates to compounds of formula (I) and to metabolites thereof.
US20080280976 Composition Comprising the Alcohol Compound Isolated from the Extract of Cucurbitaceae Family Plant Having Anti-Adipogenic and Anti-Obesity Activity The present invention is related to an alcohol compound isolated from the extract of Cucurbitaceae family plant having anti-adipogenic and anti-obesity activity, and a composition comprising the same. The compound showed potent reducing activity of body weight, decreasing effect on the blood triglyceride and cholesterol level, activating activity of PPAR α and preventing activity from the adipogenesis of precursor fat cells with no toxicity, therefore, those extract can be useful in treating or preventing obesity and adipogenesis-involved diseases as a medicine or health care food.
US20090075927 Sweet taste receptors This invention provides novel genes and polypeptides of the sweet receptor family, methods for production of the polypeptides, methods for screening compounds that specifically bind to and/or modulate the activity of these polypeptides; and antibodies specific for the polypeptides.
CN101416934A Calcium gluconate gel The invention discloses a preparation method of calcium gluconate gel, which essentially comprises the following steps: 400 portions to 800 portions of calcium gluconate, 40 portions to 60 portions of jelly powder, 10 portions of potassium sorbate, 7 portions of aspartame and 2 portions of juicy peach-taste essence are weighed; the jelly powder is added into purified water with the preparation quantity of 95 percent and the mixture is stirred at the room temperature and swells for one hour for standby; the calcium gluconate is dissolved in boiled water, cooled to the room temperature and added into the swelling solution together with the aspartame, then the mixture is stirred evenly, boiled for sterilization, added with the potassium sorbate and the essence after being cooled, stirred and dissolved, and subpackaged, thus obtaining the calcium gluconate gel. The invention aims at providing the preparation method of the calcium gluconate gel, which has exact effectiveness, stable quality, simple and easily-operated production method, convenient carrying and use, and no secondary pollution, and is favorably accepted by users.
CN101313916A Orally taken hypochlorous acid oxidization oral liquid The invention relates to a medical field, in particular to a 'hypochlorous oxidation oral liquid for oral administration'. The invention uses a strong oxidizing property of nascent oxygen generated by chemical reaction of chlorine and water to remove bacteria and viruses in human bodies. With a strong smell and a simulative property, hypochlorous, when taken orally and alone, can stimulate and cause damages to oral cavity, esophagus, gastric mucosa, etc. Therefore, hypochlorous with a concentration in a certain range can not be taken orally. The invention mainly provides a method for taking the hypochlorous. The method comprises the following steps: pouring boiling water into and fully dissolving a certain amount of brown sugar, honey, milk, etc.; when the liquid is cool enough as to not burn the mouth, adding a certain number of chlorine dissection tablets or a certain amount of bleaching powder with complete stirring; and taking orally. The brown sugar, honey, milk can protect the oral cavity, the esophagus and the gastric mucosa against the simulation of the hypochlorous and can reduce the smell of the hypochlorous. The hypochlorous oxidation oral liquid for oral administration of the invention is used to remove bacteria and viruses in the human bodies by the strong oxidizing property of the hypochlorous. With a proper dosage, the hypochlorous oxidation oral liquid for oral administration can realize the prevention and treatment of diseases with side effect caused by chlorine to the human bodies.
WO2014033631A1 N-(3-pyridyl) biarylamides as kinase inhibitors The present invention provides a compound of formula (I): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds.
CN102267952B Quinazoline compound and preparation method and application thereof The invention belongs to the technical field of antitumor medicaments and provides a quinazoline compound with a structure shown as a formula (I) or a pharmaceutically acceptable salt and a solvate thereof, wherein the definitions of R1, R2 and R3 are shown in the specifications. The invention further provides a preparation method of the quinazoline compound with the structure shown as the formula (I) or a pharmaceutically acceptable salt and a solvate thereof, a medicinal composition and application to the preparation of antitumor medicaments for treating diseases such as lung cancer, prostatic cancer, colon cancer, leukemia, breast cancer, liver cancer, stomach cancer, pancreatic cancer, human malignant glioma, brain tumor and the like.
CN103130696A Anthranilamide compound as well as preparation method and application thereof The invention relates to an anthranilamide compound shown in a formula I. The invention further provides a preparation method of the compound and an application of a composition containing the compound in preparation of antitumor medicines.
CN101947266A Solid aromatic sobering-up agent and preparation method thereof The invention discloses a solid aromatic sobering-up agent and a preparation method thereof. The solid aromatic sobering-up agent comprises the following components in percentage by mass: 0.75 to 1.50% of sobering-up essence, 0.50 to 1.50% of solid air refresher, 8.00 to 10.00% of efficient solubilizer, 0.40 to 0.60% of preservative and the balance of distilled water. The preparation method comprises the following four steps: preparing the sobering-up essence, solubilizing the sobering-up essence, preparing gel and mixing the sobering-up essence and the gel. In the invention, the essential oil such as anise oil is used as a component of the sobering-up essence, and the prepared solid aromatic sobering-up agent is an all-natural, nontoxic, harmless and safe product. Moreover, as the sobering-up agent comprises components such as lavender oil, the solid aromatic sobering-up agent emits fresh and soft smell of flowers and grass, which not only can purify air, but also has functions of removing fatigue, resisting depression and comforting mood; the sobering-up agent can consecutively emit pleasant aroma for 3 to 5 days and has no pollution to environment.
CA2223754C Actinomyces pyogenes and actinomyces pyogenes/fusobacterium necrophorum vaccines for immunizing cattle and sheep Novel inocula for administration to ruminant animals such as cattle or sheep are provided in order to immunize the animals and lessen the incidence of liver abscesses and/or foot rot therein. In one aspect, the invention pertains to an A. pyogenes-derived vaccine including an inactivated cell culture product (e.g., cell-elaborated supernatant) from A. pyogenes cell culture in a suitable carrier. In another aspect, the invention relates to a multivalent vaccine including at least first and second bacterial components in a carrier, the first component comprises an inactivated cell culture product of A. pyogenes whereas the second component comprises an inactivated cell culture product of F. necrophorum. The inocula of the present invention finds particular utility in incidences where ruminant animals are particularly subject to A. pyogenes infection leading to liver abscesses and/or foot rot, e.g., where the animals are regularly treated with an antibiotic or where cattle are fed a high grain content concentrate diet.
US20090042857 Novel Pharmaceutical A tissue-selective androgen receptor modulator containing a compound represented by the formula wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents an optionally further substituted 4- to 10-membered ring, Ring C represents an optionally further substituted benzene ring, X1 represents an optionally substituted carbon atom, X2 represents an optionally substituted carbon atom, an oxygen atom and the like, W1 represents a nitrogen atom and the like, Y11 represents a group represented by the formula CR2R3′ (wherein R2 represents a hydrogen atom, a cyano group, a nitro group and the like, and R3′ represents a bond, a hydrogen atom, a cyano group, a nitro group and the like, respectively), Y21 represents a group represented by the formula CR4R5′ (wherein R4 represents a hydrogen atom, a cyano group, a nitro group and the like, and R5′ represents a bond, a hydrogen atom, a cyano group, a nitro group and the like, respectively) and the like, R1 represents an electron-withdrawing group, and the formula represents a single bond or a double bond, or a salt thereof or a prodrug thereof.
WO2014008159A1 Selective estrogen receptor degraders for treatment of tamoxifen resistant tumors Compositions and methods for covalently bonding a polycarboxylic fatty acid and a SERD (selective estrogen receptor degrader) to form fatty acid-drug conjugate compounds are described. The conjugate compounds are useful for increasing solubility of the SERD as well as targeting the SERD to solid tumors. In particular, the compounds are surprisingly efficacious against tamoxifen-resistant tumors. These types of tumors are recalcitrant to existing therapies and often signal the end stage of cancer.
CN101743232A compounds and methods for modulating fxr Compounds of formula (I): formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and diseases related to dyslipidemia.
US20110190249 Therapeutic methods and uses of sapogenins and their derivatives The invention discloses therapeutic methods and uses of certain steroidal sapogenins, related compounds and derivatives thereof, in the treatment of non-cognitive neurodegeneration, non-cognitive neuromuscular degeneration, motor-sensory neurodegeneration or receptor dysfunction or loss in the absence of cognitive, neural and neuromuscular impairment.
WO2005005427A1 PYRROLO[3,4-c]PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS Pyrrolo[3,4-c]pyrazole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
CN102584862A Biapenem crystalline compound and composition powder-needle thereof The invention relates to a biapenem crystalline compound, which is measured by using a powder X-ray diffraction measurement method. An X-ray powder diffraction pattern indicated by a diffraction angle of 2 theta +/-0.2 degree shows feature diffraction peak at the positions of 5.9 degrees, 6.5 degrees, 10.5 degrees, 14.8 degrees, 15.6 degrees, 16.3 degrees, 17.4 degrees, 19.8 degrees, 22.9 degrees, 23.7 degrees, 25.1 degrees, 28.4 degrees and 34.7 degrees. The invention further relates to a biapenem composition powder-needle comprising the biapenem crystalline compound. Components of the composition powder-needle are 95 to 100 parts of the biapenem crystalline compound and 0.1 to 1 part of sodium benzoate.
WO2005020973A2 Compositions having antimycrobial activity including a hydroxamate or a hydroxamate and a hydroxylamine Antimycorbacterial compositions are disclosed comprising at least one hydroxamate or at least one hydroxamate and at least one hydroxylamine. The preferred ratio of hydroxamate to hydroxylamines is about 100:1 to about 1:1. A method for inhibiting mycobacterial growth is also disclosed comprising the step of administering the compositions of this invention to an animal including a human.
CN1830423A Preparation method of garlicin injection A garlicin injection for preventing and treating acute and chronic bacillary dysentery and enteritis, pertussis, fungus infection of lung and digestive tract, etc is prepared through ultrasonic treating to garlicin and tween-80, mixing with alcohol, ultrafiltration, pouring it in containers containing N2 in dark condition, sterilizing, and lamp examining.
USRE40811 Administering anti-VLA-4 antibody (or anti-VCAM-1 antibody) which blocks binding VLA-4 antigen on surface of CD34 cells to VCAM-1 or fibronectin, thereby increasing number of CD34+ cells in peripheral blood; colony stimulating factors The invention relates to in vivo peripheralization of CD34+ cells by administering anti-VLA-4 antibodies or anti-VCAM-1 antibodies.
WO2013147687A1 A nicotine oral delivery product containing a powder enclosed in a water insoluble pouch, wherein said powder comprises nicotine and a chewing gum composition The invention relates to a nicotine oral delivery product containing a powder enclosed in a water insoluble pouch, wherein said pouch is permeable for saliva and therein dissolved parts of the powder,wherein said powder comprising at least a) nicotine selected from the group consisting of tobacco, nicotine salts, nicotine base, stabilized nicotine, and mixtures thereof corresponding to 0.1 to 20 mg nicotine in the form of nicotine base and b) a chewing gum composition and a method of producing said nicotine oral delivery product.
US7063958 that encode a receptor for leptin, including a naturally occurring soluble form of the receptor that is expected to modulate, especially agonize, leptin activity; could be used to treat obesity The present invention relates to identification of a receptor for a satiety factor, which is involved in body weight homeostasis. Mutations in this receptor are associated with obese phenotypes. In particular, the present invention relates to identification and characterization of the receptor for leptin, including a naturally occurring soluble form of the receptor that is expected to modulate leptin activity, in particular to agonize leptin activity. The invention further relates to the nucleic acids encoding the receptor, and to methods for using the receptor, e.g., to identify leptin analogs, therapeutically, such as in gene therapy or in soluble form as an agonist or antagonist of leptin activity, or diagnostically.
US20090297634 Compositions for sustrained release of nitric oxide, methods of preparing same and uses thereof The invention provides compositions for releasing nitric oxide (NO) comprising a matrix that encapsulates nitric oxide. Nitric oxide is released when the composition is exposed to an aqueous environment. The invention further provides methods of preparing the compositions and uses of the compositions for treating infections and disorders.
US20120046367 Essential oil composition with anti-free radical ability Disclosed is an essential oil composition with anti-free radical ability, which includes dl-Citronellol, Eugenol, cis/trans-Citral, Eugenol Methyl Ether and Thymol. It is confirmed that the essential oil composition of the present invention has superior anti-free radical ability and anti-oxidative ability according to the indices including DPPH free radical scavenging ability, ABTS+ free radical scavenging ability, metal ion chelating ability and reducing property, which are extensively used to determine the anti-oxidative ability of a substance.
EP2731938A1 Novel anti-cancer isocarbostyril alkaloid conjugates The present application is directed to covalent conjugates between an isocarbostyril alkaloid and a lipophilic biomolecule, to pharmaceutical compositions comprising the conjugates and to therapeutic uses thereof, in particular for treating cancer.
WO2005099486A1 Process for preparing lagerstroemia speciosa l. extract A process for preparing an Lagerstroemia speciosa L. extract of low bitterness comprising, contained in Lagerstroemia speciosa L. as a blood sugar level increase inhibiting component, corosolic acid or corosolic acid plus ellagitannin in high proportion. This process comprises the steps of (1) extracting Lagerstroemia speciosa L. with a hydrous organic solvent, concentrating the obtained extract and dispersing the concentrate in a hydrous organic solvent, (2) subjecting the dispersion to solid/liquid separation and performing fractionation into an insoluble matter and a soluble matter, (3) extracting the insoluble matter with an alkali hydrous organic solvent and collecting the extract, and (4) treating the extract with an acid and collecting precipitates.
WO2009048868A1 Photodynamic therapy process and photosensitizer compositions Use of a photosensitizer composition in the manufacture of a medicament for photodynamic therapy and a process for photodynamic therapy are provided along with a photosensitizer composition suitable for the use and the process. The photosensitizer composition comprises at least one photoactive ingredient in a chemically reduced state. According to the use, the photosensitizer composition having at least one photoactive ingredient in a chemically reduced state is provided. The photosensitizer composition is applied to tissue or other substrate such that the at least one photoactive ingredient is at or travels to a location adjacent a target medium and the at least one photoactive ingredient is then altered to a photoactive state. The at least one photoactive ingredient is then exposed to light energy for assisting in inhibiting at least one pathogen at the target medium. The prefered photosensitizer is methylene blue. It is preferably reduced by ascorbic acid.
US20100278905 Stabilized lipid formulation of apoptosis promoter An orally deliverable pharmaceutical composition comprises a Bcl-2 family protein inhibitory compound, e.g., ABT-263, a heavier-chalcogen antioxidant and a substantially non-aqueous lipid carrier, wherein said compound and said antioxidant are in solution in the carrier. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
CN103254259A Iridoid glycoside compound as well as preparation method and application thereof The invention discloses an iridoid glycoside compound as well as a preparation method and an application thereof. The preparation method of the iridoid glycoside compound comprises the following steps of: (1), taking a reduning injection finished product for HP-20 macroporous adsorption resin column chromatography separation, carrying out gradient elution by water, 30% alcohol and 90%-100% alcohol in sequence, collecting and concentrating eluant to obtain a 90%-100% alcohol elution part; and (2), carrying out silica gel column chromatography, ODS (Ozone Depleting Substances) column chromatography separation, semi-preparation liquid phase HPLC (High Performance Liquid Chromatography) separation in sequence to obtain the iridoid glycoside compound. The iridoid glycoside compound disclosed by the invention can be used for treating hand-foot-and-mouth diseases.
US20100247461 Anti-inflammatory complexes Disclosed are certain complexes of AFC compounds and binding agents. Such complexes are useful, among other things, in the treatment of inflammatory diseases or disorders.
EP1609482A1 Drug for treating hemophilia and method of treating hemophilia using the same A therapeutic product or drug for therapy of hemophilia may be produced by a simplified method including embedding genes of the blood clotting factors VIII (IX) for therapy of hemophilia in hollow nano particles obtained on expressing the protein having a particle forming function, such as hepatitis B virus surface antigen protein, in eucaryotic cells. The drug so produced is able to introduce the genes of the blood clotting factors efficaciously into liver cells with the least risk of side effects.
CN103626693A A class of pleuromytilin derivatives, drug composition, synthesis methods and uses thereof The present invention relates to a class of pleuromytilin compounds represented by the following general formula (I), pharmaceutically acceptable salts and preparation methods thereof, and compositions comprising the compound represented by the general formula (I) as an active component. The compounds have excellent antibacterial activities and can be adopted as the active substance for infectious disease treatment.
US20050222125 For therapy of depression, anxiety and body weight disorders The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2 and R3 are certain specific substituents, with the proviso that at least one of R1 and R2 is an amino radical of formula N—R10R11 wherein R10 and R11 are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonin (5-HT) reuptake inhibitor activity in combination with additional α2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention are also suitable for treating depression, anxiety and body weight disorders. The invention also relates to novel combination of substituted amino isoxazoline derivatives according to the invention with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action.
US8076347 (-)-(2S,4S)-1-(2-hydroxymethyl-1,3-dioxolan-4-yl)cytosine (OddC); "L"-nucleoside that exhibits anti-tumor activity; anticarcinogenic agent for non-small cell lung cancer, colon, breast, prostate, ovarian, CNS, renal, and lymphoma cancer, leukemia, melanoma (−)-(2S,4S)-1-(2-Hydroxymethyl-1,3-dioxolan-4-yl)cytosine (also referred to as (−)-OddC) or its derivative and its use to treat cancer in animals, including humans.
CN1857264A Medicine composition with pioglitazone hydrochloride and glimepiride as active components and its preparing method and use The present invention relates to a kind of medicine composition with pioglitazone hydrochloride and glimepiride as active components and its preparation process and use. The medicine composition is used for treating type II diabetes. Pioglitazone hydrochloride and glimepiride as active components and certain amount of supplementary material are prepared into tablet, capsule, dispersant tablet, chewing tablet and other orally taken preparations.
US7109213 Aminopiperidine compounds, process for their preparation, and pharmaceutical compositions containing them Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
WO2004087713A8 Salts of tricyclic inhibitors of poly(adp-ribose) polymerases Pharmaceutically acceptable salts of compounds of the formula (I) below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.
US20100197617 Process for the preparation of caralluma extract and a formulation prepared thereof Processes for the preparation of Caralluma extract which includes shade-drying of Caralluma plant material; ii) treating the dried Caralluma plant material by at least one operation selected from a group consisting of sorting, cleaning and sizing to obtain Caralluma plant material meant for extraction or any combination thereof; iii) extracting the Caralluma plant material with a first solvent for at least two initial iterations followed by at least two subsequent iterations with a second solvent at controlled temperature to obtain a diluted extract; iv) removing the solvent from the diluted extract by distillation at a temperature below about 40° C. to obtain a concentrate; v) chilling the concentrate at a temperature of about 6 to about 10° C. for a period of about 7 to about 8 hours to obtain a chilled concentrate; vi) filtering the chilled concentrate to obtain a filtrate; vii) concentrating the filtrate at a temperature below about 60° C. to obtain a viscous liquid; viii) spray-drying the concentrated viscous liquid to obtain a powder; and ix) pulverizing and sifting the dried powder to obtain a Caralluma extract provided. Such extracts may be included in medicinal formulations used for the prevention and treatment of obesity and obesity-related conditions for subjects in need thereof.
WO2012089876A1 Pyrimidine urea‑derived compound for treating inflammatory diseases The present invention relates to a pyrimidine urea‑derived compound for treating inflammatory diseases. The compound of the invention can be used for preparing a pharmaceutical composition for treating said inflammatory diseases, preferably sepsis caused by Gram‑negative bacteria, arthritis, renal infections, acute sepsis‑induced pulmonary diseases, acute sepsis‑induced respiratory distress syndrome, endotoxic or endotoxemic shock, septic peritonitis, acute hepatitis, acute septic‑shock‑induced myocardial dysfunction and necrotizing enterocolitis.
CN103006671A Application of vitamin D3 in preparation of medicine for preventing dairy cow mastitis The invention provides application of a vitamin D3 in preparation of a medicine for preventing dairy cow mastitis. Active components of the medicine comprise the vitamin D3 and one or more antibiotics, and 10g of medicine is applied to every dairy cow each day. The medicine has a good and remarkable preventing effect for the dairy cows in a lactation period and a dry period without toxic and side effects, and can avoid loss for curing the diseased dairy cows.
WO2014012090A1 Molecular sleds comprising a positively-charged amino acid sequence and a molecular cargo and uses thereof The present invention relates to compositions which may comprise a molecular sled linked to cargo and uses thereof. In particular, the present invention relates to a non-naturally occurring or engineered composition which may comprise a molecular sled, linkers and a molecular cargo connected to the sled via the linkers. Methods involving the use of molecular sleds and their cargoes and pharmaceutical compositions, methods for treating treating cancer, a degenerative disease, a genetic disease or an infectious disease as well as diagnostic methods are also contemplated by the present invention.
WO2005121132A1 Fused heterocyclic compound having anti-hcv effect Disclosed is a compound represented by the formula (I) below, a pharmaceutically acceptable salt thereof, or a solvate of them. (I) (In the formula, A represents N or CH; Het represents any one of the following groups: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k) wherein R0 and R respectively represent a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted aryl or the like; R1 and R2 respectively represent a hydrogen, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl or the like; p is an integer of 0-3; and R3 represents an optionally substituted alkyl or the like.)
US7151109 Psychological disorders; anxiolytic agents; antidepressants The present invention relates to novel pyrazolo[1,5-a]pyridine derivatives of general formula I: that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety disorders, and depression and stress related disorders.
CN102247358A Novel application of 3,3'-di(5,6-dioxindole)methane The invention belongs to the field of radiation damage protection medicament, and relates to a novel application of 3,3'-di(5,6-dioxindole)methane in the preparation of radiation damage protection medicament. The structural formula of 3,3'-di(5,6-dioxindole)methane is presented as the following. 3,3'-di(5,6-dioxindole)methane provided by the invention can be applied in the preparation of radiation damage protection medicament. With a low density which brings no toxic and side effect, the medicament assists in improving cell survival rate after the cells are irradiated by ionizing radiation.
CN102526016A Application of 5,8-dyhydroxyl-2-(1-acetyl-4-methyl-3-pentenyl)-1,4-naphthoquinone diketone to preparation of medicines for resisting diabetes The invention relates to application of 5,8-dyhydroxyl-2-(1-acetyl-4-methyl-3-pentenyl)-1,4-naphthoquinone diketone, namely acetylshikonin to the preparation of medicines for treating type I and type II diabetes. Experiments prove that the substance has an effect of reducing blood sugar by insulin-like, has a superimposed effect with a blood sugar reducing effect of insulin and has a synergistic effect with the blood sugar reducing effect of dimethyldiguanide, so the 5,8-dyhydroxyl-2-(1-acetyl-4-methyl-3-pentenyl)-1,4-naphthoquinone diketone can be prepared into compound preparations with blood sugar reducing medicines such as the insulin, the dimethyldiguanide and the like.
EP1246827B1 New polymorphic forms of olanzapine The invention provides three new polymorphic forms of 2-methyl-4-[4-methyl-1-piperazinyl]-10H-thieno[2,3b][1,5] benzodiazepine (Olanzapine) (Formula A), the process for preparing the new polymorphs and pharmaceutical compositions containing the polymorphs. The new polymorphic forms of olanzapine are useful for the treatment of psychotic conditions, mild anxiety and gastrointestinal conditions.
WO2005034945A1 Use of norphenazone and coenzyme q for curing arthrose, arthritis and osteoarthritis The invention relates to a pharmaceutical preparation containing norphenazone (3-methyl-1-phenyl-2-pyrazolin-5-one) or the pharmaceutically acceptable salts thereof or coenzyme Qn (N ranging from 6 to 10) or the mixture of the components thereof which is very efficient for therapeutically curing arthrose, arthritis and osteoarthritis and for prophylactics during interventions on articulations. The inventive preparation is particularly useful for any surgical intervention on articulations, in particular for arthroscopies and for above-mentioned diseases. Said preparation reduces the Chondrocytes destruction in affected tissues and the degradation of a polymeric matrix encompassing the Chondrocytes of the related articulation cartilage.
US7078436 Administering halosubstitured phenyl alkyl carbamate compound for therapy of anxiety This invention is directed to a method for preventing or treating anxiety disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).
EP2678349A1 C-4" position substituted macrolide derivative A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas).
CN102048733A Medicinal use of nalmefene hydrochloride The invention relates to medicinal use of nalmefene hydrochloride. The nalmefene hydrochloride can improve lipid metabolism and improve prognosis of a fatty liver patient by reducing the platelet aggregation rate, improving the liver function state and resisting oxidation. The nalmefene hydrochloride can serve as a medicine for resisting human/animal fatty liver.
CN101693705B Phenol compound as well as preparation method and applications thereof The invention discloses a phenol compound as well as a preparation method and applications thereof. The structural formula of the phenol compound is shown as formulas (I) to (III), wherein a compound shown in the formula (I) is ito1ideA, a compound shown in the formula (II) is ito1ideB, and a compound shown in the formula (III) is itosideP. The preparation method of the compounds comprises the steps of extracting the collected plant itoa orientalis branch leaves and tree barks with organic solvent after drying and crushing, then obtaining a paste-shaped extract by decompression and concentration of the extract liquid, separating and purifying the paste-shaped extract, and the like. The phenol compound has good activity, can be used in the preparation of insecticides, acaricides, fungicides or herbicides and can also can be used in the preparation of anti-virus or anti-cancer drugs.
CN102961398A Gastric acid stimulation-reducing anti-thrombus and anti-coagulation composite and preparation method The invention discloses an anti-thrombus aggregation and anti-coagulation compound preparation able to reduce gastric acid stimulation. The compound preparation is characterized by being prepared from 2-180 parts of aspirin, 10-50 parts of heavy magnesium carbonate, and 5-30 parts of Dihydroxyaluminium Aminoacetate, wherein the aspirin and the alkaline drug heavy magnesium carbonate, Dihydroxyaluminium Aminoacetate are at different inner and outer layers. At the same time, an inclusion material is used in the aspirin layer and a buffer layer to prepare an inclusion compound, thus solving the problem of isolating the aspirin layer (acidic drug) from the alkaline drugs to prevent reaction during preparation, and also solving the reaction problem of the acidic drug and the alkaline drugs after the compound preparation enters the stomach by oral taking. The alkaline drugs can neutralize gastric acid so as to improve gastric acid increase, direct stimulation on gastric mucosas, epigastric pain and other clinical symptoms. The alkaline drugs also can accelerate gastric emptying, and make aspirin quickly enter the small intestine to speed up absorption. The invention simultaneously discloses application of the compound preparation in preparation of anti-platelet aggregation or anti-coagulation drugs, especially in preparation of drugs treating unstable angina pectoris, acute myocardial infarction, ischemic cerebrovascular disorder and other aspects.
US7459142 High viscosity embolizing compositions comprising prepolymers Disclosed are novel high viscosity compositions for embolizing blood vessels which comprise a biocompatible prepolymer and a contrast agent, and optionally a thickening agent and/or a biocompatible solvent. Also disclosed are methods for embolizing a vascular site by injecting high viscosity prepolymer compositions into said site. The disclosed compositions and methods are particularly well suited for the treatment of aneurysms.
CN102085258B Cream preparation for preventing and curing mammary gland hyperplasia and preparation method thereof The invention discloses a cream preparation for preventing and curing mammary gland hyperplasia and a preparation method thereof. The cream preparation comprises the active constituents of flos rosae rugosae, syzygium aromaticum, rhizoma corydalis, cowherb seeds, garden balsam stems, rheum officinale, musk and borneol. The preparation method comprises the following steps of: extracting the flos rosae rugosae, the syzygium aromaticum, the rhizoma corydalis, the cowherb seeds, the garden balsam stems and the rheum officinale through an alcohol solution, and leaching the solution to remove alcohol to obtain a filter liquor; decocting medicine dregs with water to obtain a decoction liquor; combining the filter liquor and the decoction liquor to obtain a drug extract; uniformly mixing the drugextract with a substrate; and then adding the borneol and the musk to obtain the cream preparation for preventing and curing the mammary gland hyperplasia. The cream preparation has the advantage of precise and appropriate compatibility and the effects of smoothing the liver, relieving stasis, promoting the flow of qi and blood circulation, eliminating stagnations and stopping pains, can obviously control the mammary gland hyperplasia, reduce and regulate the contents of estrogen and progesterone in the blood and down regulating the expression of mammary gland hyperplasia tissues AP-2alpha and C-erbB-2 so as to achieve the purposes of treating the mammary gland hyperplasia and preventing breast cancer.
CN1849302A 1, 3-disubstituted azetidine derivatives for use as CCR-3 receptor antagonists in the treatment of inflammatory and allergic diseases Compounds of formula Ia or Ib in free or salt form, wherein Ar, X<1>, X<2>, m, R<1>, Q, Y, R<2> and R<3> have the meanings as indicated in the specification, are useful for treating conditions that are mediated by CCR-3, for example an inflammatory or allergic condition, particularly an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
CN102558187A Tetrahydroporphin compound and preparation method and application thereof The invention relates to a tetrahydroporphin compound and a preparation method and an application thereof. The structural formula of the compound is shown in the specifications. The preparation method comprises the following steps of: synthesizing 2,3-dihydro-2,3-di(dicyan methyl)-5,10,15,20-tetraphenyl porphin; synthesizing 2,3-dihydro-2,3-di(dicyan methyl)-12-nitro-5,10,15,20-tetraphenyl; synthesizing 2,3-cis-12,13-tetralin-2,3-di(dicyan)-[12:13]-[di(methoxycarbonyl group), di(cyan)methylene]-5,10,15,20-tetraphenyl; and synthesizing 2,3-cis-12,13-tetralin-2,3,12,13-(tetra-carboxymethyl)-5,10,15,20-tetraphenyl porphin. The tetrahydroporphin compound is applied to the preparation of a photosensitizer medicament for treating tumor diseases, and has a definite structure and a wide application prospect, and is easy to prepare.
US6872853 Bioavailability; reacting sertratineamine with hydrogen chloride A cystalline form of sertraline hydrochloride was found, referred to hereinafter as polymorphic form CSC2 having a dissolution rate which surprisingly will increase rate of absorption of a drug. Furthermore, different crystalline forms of sertraline hydrochloride alcohol solvates, crystalline forms of sertraline hydrochloride hydrates, referred to hereinafter as polymorphic form CSC1, a process for the preparation of the amorphous form of sertraline hydrochloride, and different processes for the preparation of polymorphic forms I, II, V, and T1 are disclosed.
WO2014159171A1 Methods of treating lung cancer The present invention provides methods and compositions for treating non-small-cell lung cancer (NSCLC) by administering a) a composition comprising nanoparticles that comprise paclitaxel and an albumin and b) a platinum-based agent (e.g., carboplatin), wherein the individual has diabetes, has four or more metastatic sites, and/or is at least about 70 years old.
US20120220560 Steroid tetrol solid state forms The invention relates to solid state forms of androst-5-ene-3β,7β,16α,17β-tetrol, formulations containing or prepared from such solid state forms and use of these materials for modulating unwanted inflammation including acute and chronic non-productive inflammation. The formulations can be used to prevent, treat or slow the progression of conditions related to autoimmunity and metabolic disorders such as arthritis, multiple sclerosis, ulcerative colitis, Type 1 diabetes and Type 2 diabetes.
CN102210673A Cyclodextrin inclusion compound containing ligustilide, and preparation method thereof The invention provides a cyclodextrin inclusion compound containing ligustilide, comprising ligustilide and hydroxypropyl-beta-cyclodextrin, wherein the ligustilide is included in the hydroxypropyl-beta-cyclodextrin to form an inclusion compound, the percentages by weight of the ligustilide and the hydroxypropyl-beta-cyclodextrin are 10-20%, and the cyclodextrin inclusion compound further contains povidone K29/32 which accounts for 10-50% of the hydroxypropyl-beta-cyclodextrin by weight. The cyclodextrin inclusion compound containing the ligustilide can be prepared into tablets, capsules, powder or powder injections as medicaments for treating dysmenorrhea.
US20120028930 Flupirtine salts and polymorphs The present invention includes salts and polymorphs of flupirtine including, but not limited to carboxylic acid salts and sulfonic acid salts and their polymorphs. The present invention also includes pharmaceutical compositions comprising the salts and polymorphs of flupirtine. The invention also relates to the therapeutic use of the flupirtine salts and polymorphs to treat nervous system disorders, pain disorders, musculoskeletal disorders, and other diseases and conditions.
US20110003761 Biologically active extract from dendrobium plant, use thereof and process for preparing the same A substance having the following formula is provided. wherein R1 and R2 are selected from a group consisting of α-Arabinose, β-Arabinose and β-Xylose. The substance has an effect of accelerating a phagocytosis of RPE.
US20050222268 Administering a compound for inhibiting cation exchange as hypotensive agents A therapeutic agent for hypertension, which comprises as an active ingredient a compound capable of inhibiting Na+/Ca2+ exchanger 1.
US20100158989 Hemostatic Agent Composition, Delivery System and Method A hemostatic agent composition, delivery system and method include a hemostatic agent composition which is inert and non-reactive relative to blood clotting proteins and platelets. The composition includes a clay material combined with a humectant in a stable suspension embedded in a mesh fabric and, when dried, is capable of accelerating the formation of a stable clot when applied to an actively bleeding wound or drying other bodily fluids.
CN102796087A Coumarin triadimenol, and preparation method and application thereof The invention discloses coumarin triadimenol shown in a structural formula I and a preparation method thereof. The preparation method comprises the following step: under the catalytic effect of inorganic base, reacting 5,7-di((epoxyethyl-2-)methoxy)-4-methyl coumarin and 1H-1,2,4-triazole at 60-80 DEG C in an organic solvent while stirring. In-vitro antimicrobial activity detection discovers that the compound has a certain activity inhibition effect on gram positive bacteria (Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Micrococcus luteus and Bacillus subtilis), gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Bacillus proteus and Salmonella typhosa) and fungi (Candida albicans and Candida krusei). The compound can be used for preparing antibacterial and/or antifungal drugs.
CN1846680A Slow-released methotrexate injection The slow released methotrexate injection consists of slow released microballoon and solvent. The slow released microballoon includes effective anticancer component and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The suspending agent is sodium carboxymethyl cellulose, mannitol, sorbitol, Tween-80 or their composition. The effective anticancer component is methotrexate or the composition of methotrexate and its synergist of caryocinesis regulating medicine and/or alkylating agent; and the slow releasing supplementary material is PLA, PLGA, EVAc, etc or their composition. The slow released microballoon may be also prepared into slow released implantation preparation. Implanting or injecting the slow released preparation to local tumor part can lower the systematic toxic reaction of the medicine and raise the medicine concentration of local tumor part selectively to raise the treating effect.
WO2006080582A1 Agent for control of function of antigen-presenting cell Disclosed is an agent for controlling the function of an antigen-presenting cell. An agent for controlling the function of an antigen-presenting cell comprising, as an active ingredient, a substance capable of controlling the concentration of zinc ions in a cell, specifically a zinc ion, a zinc-ion chelator, a substance capable of controlling the expression and/or function of a zinc ion-requiring protein or a substance capable of controlling the expression and/or function of a zinc ion transporter.
WO2012031773A1 Sdf-1 binding nucleic acids and the use thereof in cancer treatment The present invention is related to a nucleic acid molecule capable of binding to SDF-1, preferably capable of inhibiting SDF-1, whereby the nucleic acid molecule is for use in a method for the treatment and/or prevention of a disease or disorder, for use in a method for the treatment of a subject suffering from a disease or disorder or being at risk of developing a disease or disorder as an adjunct therapy, or for use as a medicament for the treatment and/or prevention of a disease or disorder, whereby the disease or disorder is cancer.
WO2008098485A1 The salts of 4-aniline quinazoline derivative The salts of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazoline-6-yl}- acrylamide, preparation methods, compositions containing the same and their uses thereof. The present salts have excellent anti-tumour activity, good bioavailability in vitro and in vivo in animals and low toxicity, so they are suitable for anti-tumour medicaments.
WO2013009910A3 Eosinophil peroxidase compositions and methods of their use Eosinophil peroxidase compositions and methods of their use for preventing and/or inhibiting the growth of susceptible microorganisms. The compositions include an eosinophil peroxidase, a peroxide or peroxide source, and at least two amino acids.
EP0863903B1 Synthetic metal-substituted bacteriochlorophyll derivatives and use thereof Metalated bacteriochlorophylls of the formula [M]-BChl, wherein M is a metal atom selected from divalent Pd, Co, Ni, Cu, Zn and Mn, trivalent Fe, Mn and Cr, and tetravalent Sn and Pt, and Bchl represents the residue of a demetalated natural or synthetic bacteriochlorophyll derivative, are prepared by transmetalation of the corresponding [Cd]-BChl derivatives carrying at position 173 a group COOR¿1?, wherein R1 is a C1 - C25 hydrocarbyl residue, and further optional transesterification of the 17?3-COOR¿1 of the obtained [M]-BChl. The compounds are for use in photodynamic therapy and diagnosis and for killing cells and infectious agents, e.g. bacteria and viruses, both in biological products and in living tissue. Preferred compounds are those of formula (I') wherein R'1 is a residue selected from (i) optionally substituted hydrocarbyl; (ii) hydroxy-containing amino acid or peptide or a derivative thereof; and (iii) hydroxy-containing peptide or a cell-specific ligand, e.g. peptide or protein, linked to the COO-group via a spacer as defined in (i).
EP2327451A2 Method for detecting and inhibiting angiogenesis The present invention provides methods for reducing or inhibiting angiogenesis in a tissue, by contacting α5β1 integrin in the tissue with an agent that interferes with specific binding of the α5β1 integrin to a ligand expressed in the tissue; and methods of identifying angiogenesis in a tissue, by contacting the tissue with an agent that specifically binds α5β1 integrin, and detecting specific binding of the agent to α5β1 integrin associated with a blood vessel in the tissue. Also provided are methods of diagnosing a pathological condition characterized by angiogenesis in a tissue in an individual. The invention further provides methods of reducing or inhibiting angiogenesis in a tissue in an individual, by administering to the individual an agent that interferes with the specific binding of α5β1 integrin to a ligand expressed in the tissue; and methods of reducing the severity of a pathological condition associated with angiogenesis in an individual, by administering to the individual an agent that interferes with specific binding of α5β1 integrin to a ligand in a tissue associated with the pathological condition. The invention also provides methods of identifying an agent that reduces or inhibits angiogenesis associated with α5β1 integrin expression in a tissue by contacting a tissue exhibiting angiogenesis associated with α5β1 integrin expression with an agent, and detecting a reduction or inhibition of angiogenesis in the tissue.
US20120022009 Tannate dry powder formulations Dry powder tannate compositions containing bioactive agents, tannic acid, dispersants, and viscosity modifying agents are disclosed. Specifically, the bioactive agents are antihistamines, decongestants, antitussives, and anticholinergics. The dry powder formulations can further include pharmaceutically acceptable excipients. The dry powder formulations exhibit increased stability for extended shelf life. Bioactive agent tannate salts remain suspended for at least two weeks following formation of the suspension in a pharmaceutically acceptable aqueous liquid.
US20110136815 Solid oral film dosage forms and methods for making same Improved pharmaceutical solid oral film dosage forms for the buccal and/or sublingual delivery of pharmaceutical, nutraceutical or cosmetic ingredients are endowed with instant hydration potential and complete dissolution potentially enabling the active ingredient to become immediately available for enhanced buccal and/or sublingual absorption and/or reduced absorption through the gastrointestinal route. The improved delivery systems for solubilizing and stabilizing pharmaceutically active ingredients exhibit enhanced stability by the use of a combination of crystallization inhibitors, which together can maintain the active ingredient in a desired plurality of particles in an effective size range within a polymeric film matrix.
CN101883577A Combination therapy for pancreatic cancer using an antigenic peptide and chemotherapeutic agent Described herein is a combination therapy suited to the treatment of pancreatic cancer and the like. Also described is a method of potentiating the therapeutic effect of chemotherapeutic agents such as gemcitabine.
CN101941996A Ursolic acid saponin, preparation method thereof and application in resisting highly pathogenic H5N1 influenza virus The invention discloses ursolic acid saponin, a preparation method thereof and application in resisting highly pathogenic H5N1 influenza virus, and specifically relates to ursolic acid saponin compounds shown in general formula (I). A series of ursolic acid saponin is prepared from natural product ursolic acid serving as raw material by introducing an ester group into the C-28 site through structural modification at first, then introducing beta-glucosyl into the C-3 site, selectively protecting 3,6-OHs of the glucose by using BBTZ and introducing glycosyl into 2,4-OHs of the glucose. Pharmacological test shows that the ursolic acid saponin compounds have obvious inhibition effect on the invasion process of the H5N1 highly pathogenic influenza viruses on host cells and can be used as a medicament for preventing or treating the influenza viruses. The invention also discloses a pharmaceutical composition containing the ursolic acid saponin compounds and the combination of the compounds of the invention and other anti-virus medicines.
WO2013103317A1 Quinoline compounds which are anti-angiogenic integrin alpha5 betal inhibitors for use in the treatment of fibrosis or fibrosis-related diseases A new medical therapy, and more particularly certain quinoline compounds which are anti-angiogenic integrin aplha5beta1 inhibitors, for use in the treatment of fibrosis, or a fibrosis-related disease, such as a fibrotic disease affecting the lung, liver, kidney, skin, epidermis, endodermis, muscle, tendon, cartilage, heart, stomach, large intestine, small intestine, colon, uterus, nervous system, testis, adrenal gland, artery, vein, biliary tract, or eye.
CN102512420A Officinal composite using Rebamipide officinal salt as active ingredient The invention discloses an officinal composite using a Rebamipide officinal salt as an active ingredient, wherein the officinal salt comprises choline salts, arginine salt, heme-L-lysinate, trometamol salt, sodium salt, calcium salt, zinc salt, magnesium salt and the like. The Rebamipide officinal salt can be combined with a pharmaceutic adjuvant to produce solid preparations, wherein the solid preparations comprise particles, tablets, capsules, chewable tablets, orally distegrating tablets, effervescent tablets, dispersible tablets, sustained-release tablets, sustained-release capsules and the like; the Rebamipide officinal salt also can be combined with the pharmaceutic adjuvant to produce liquid preparations, wherein the liquid preparations comprise eye drops and the like; and the Rebamipide officinal salt is used for treating peptic ulcer and dry eye syndrome.
CN101507724A Use of pyrroloquinoline quinine in antiradiation The invention relates to application of pyrroloquinoline quinone in radioresistance, in particular to application of an active ingredient of the pyrroloquinoline quinone in preparing a substance used for improving the radiation resistance of an object and lightening or eliminating the influence of the radiation on the object, wherein the active ingredient of the pyrroloquinoline quinone is selected from one or more of the pyrroloquinoline quinone, and bromatologically, hygienically or pharmaceutically acceptable salt and/or ester of the pyrroloquinoline quinone. The substance has remarkable effect on the radioresistance, and has the advantages of having low toxic side effect, supplementing ingredients needed by human bodies and the like.
CN101229135A Injectio natarii norcantharidatis freeze-dried powder for injection and preparing method thereof The invention relates to a freeze-dried powder of sodium norcantharidin for injection and a preparation method for the freeze-dried powder: adding the norcantharidin and mannitol into well prepared sodium hydroxide solutions and adjusting the ph; adding activated carbon and removing colors, filtering and removing the carbon and finely filtering through a 0.22Mu m filtering film and making loading separately; cooling the separately loaded medical solution rapidly to minus 60 to minus 55 DEG C with the speed of 15 to 25 DEG C per minute; preserving heat and freezing for 3 hours and pumping the vacuum of 5 to 15 Pa; heating slowly and uniformly to minus 5 to 5 DEG C with the speed of 3 to 3.5 DEG C per hour and preserving the heat for 2 to 5 hours and then heating with a uniform speed to 20 to 30 DEG C with 3 to 6 heating hours; preserving heat and drying for 5 hours and detecting, pressing a whole cover and packaging and warehousing. The freeze-dried powder obtained by the method is high in purity, beautiful in appearance and low in water content and the proportion of the nor cantharidin, the sodium hydroxide and the mannitol is provided as 2 to 1 to 20.
WO2009133834A1 Keto-amide derivative having inhibitory activity on endothelial lipase Disclosed is a pharmaceutical composition having an inhibitory activity on endothelial lipase, which comprises a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the compound or the pharmaceutically acceptable salt. (In the formula, the ring A represents a substituted or unsubstituted heteroring, provided that the ring A may be substituted by a group other than a group represented by the formula –R1-R2-R3-R4 or the formula –X-Y-N(R5)-R6-R7-R8; X and Y independently represent –C(=O)- or –C(OH)2-; R1, R3 and R6 independently represent a single bond, a substituted or unsubstituted alkylene, or the like; R2 and R7 independently represent a single bond, -C(=O)- or the like; R5 and R9 independently represent a hydrogen or the like; and R4 and R8 independently represent a hydrogen or the like.)
WO2010047108A1 Calicivirus inactivation method Disclosed is a method which is not hazardous unlike an aqueous sodium hypochlorite solution and can effectively deactivate or inactivate a calicivirus (e.g., a norovirus) contained in a material to be sterilized even in the co-presence of an organic material mainly composed of a protein. Specifically disclosed is a method for inactivating a calicivirus in the co-presence of a protein, which comprises contacting a material which is suspected of containing a calicivirus and contains a protein with a composition which comprises an aqueous solution containing ethanol and an acid as active ingredients and having pH 2.5 to 5.0. The calicivirus is, for example, a norovirus.
CN1868475A Nasal cavity nebula contg. scopolamine hydrobromide A nasal spray of hyoscine hydrobromate is prepared from hyoscine hydrobromate, solvent, stabilizer, antiseptic and isotonic regulator. Its preparing process is also disclosed.
EP1513808A2 Fluorinated cyclic amides as dipeptidyl peptidase iv inhibitors The invention relates to new therapeutically active and selective inhibitors of the enzyme dipeptidyl peptidase-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for treating diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, hyperglycemia, impaired glucose tolerance, metabolic syndrome (Syndrome X or insulin resistance syndrome), glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inflammatory bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of identifying an insulin secretagogue agent for diabetes.
CN100594917C Externally applied medicine for curing psoriasis and producing method thereof The invention relates to a medicine for curing psoriasis and a preparation method thereof. The compound comprising components such as cantharis, chilopod, Cicada Slough, scorpion, fresh kusnezoff monkshood root, fresh common monkshood mother root, pricklyash peel and borneol and so on is socked through alcohol with a concentration of 70 percent for 7 to 12 days; the solid components are filtered out to obtain the liquid; and the liquid is the topical medicine for curing the psoriasis. The medicine of invention for curing the psoriasis has the advantages of good curing effect and quick result.
WO2007094497A1 Ameliorating agent for metabolic syndrome Disclosed is an ameliorating or prophylactic agent for metabolic syndrome, which comprises, as an active ingredient, at least one triterpene selected from the group consisting of corosolic acid, a corosolic acid analogue and pharmaceutically acceptable salts of corosolic acid and the analogue. The ameliorating or prophylactic agent can prevent hyperglycemia, hypertension, obesity, hyperlipemia and the like to thereby ameliorate or prevent metabolic syndrome. The ameliorating or prophylactic agent produces no adverse side effect when administered to a living body and therefore is extremely safe.
US8273353 Inhibitors of vascular endothelial growth factor activity The present invention is directed to novel chimeric VEGF receptor proteins comprising amino acid sequences derived from the vascular endothelial growth factor (VEGF) receptors flt-1 and KDR, including the murine homologue to the human KDR receptor FLK-1, wherein said chimeric VEGF receptor proteins bind to VEGF and antagonize the endothelial cell proliferative and angiogenic activity thereof. The present invention is also directed to nucleic acids and expression vectors encoding these chimeric VEGF receptor proteins, host cells harboring such expression vectors, pharmaceutically acceptable compositions comprising such proteins, methods of preparing such proteins and to methods utilizing such proteins for the treatment of conditions associated with undesired vascularization.
CN102078289A Cream for promoting tissue regeneration and astringing wound and preparation method thereof The invention relates to a cream for promoting tissue regeneration and astringing wound and a preparation method thereof. The cream disclosed by the invention can more favorably exert curative effect on the basis of the traditional powder and is more convenient for application.
CN102247375B Cefotetan disodium for injection, and preparation method thereof The invention relates to cefotetan disodium for injection, and a preparation method thereof. The cefotetan disodium for the injection is prepared from cefotetan, sodium bicarbonate, dilute hydrochloric acid and water for the injection, wherein the use amount of the sodium bicarbonate is 24.5-28.5% of the use amount of the cefotetan, preferably, 26.5%. The invention further provides the cefotetan disodium for the injection prepared from the cefotetan crystal, and the preparation method thereof. The cefotetan disodium for the injection provided by the present invention has good stability, smallrelated substance content, such that the potential safety hazard problem due to large impurity content is avoided; the cefotetan disodium prepared from the cefotetan crystal provided by the present invention has good stability and small related substance content, meanwhile, because the prepared cefotetan disodium contains the cefotetan crystal, the prepared cefotetan disodium has strong antibacterial characterization.
CN103623353A Medicine for treating catarrhal conjunctivitis and preparation method thereof The invention discloses a medicine for treating catarrhal conjunctivitis and a preparation method thereof. The medicine is mainly prepared from the following medicines according to a certain weight ratio: asarum sieboldii, chrysanthemum, cicada slough, burdock, fructus kochiae, pipewort and lygodium japonicum. The medicine has the effects of clearing away heat and toxic materials, clearing liver and improving vision, inducing diuresis to alleviate edema and the like, is fast in effectiveness in treatment of catarrhal conjunctivitis, good in curative effect and is free from any toxicity or side effects.
CN101259136A Acne therapeutic agent The invention discloses an acne therapeutic agent, which is invented to solve the poor acne therapeutic effect of the prior art. The main materials consist of the following drugs by weight percentage: 81.5 percent of metronidazole or Erythromycin, 4 percent of cillimycin, 3 percent of lidocaine, 10 percent of ketoconazole, 0.3 percent of clobetasol propionate and 1.5 percent of moroxydinehydro chloride or ribavirin; the ratio scope of any of the above drugs does not exceed or be lower than 85 percent of specific gravity of the drug. The acne therapeutic agent prepared from the above ingredients has such functions as antianaerobic effect, antifungal effect, oil controlling and antiviral effect, and can inhibit the synthesis of DNA of bacteria, so as to interfere growth and proliferation of bacteria and result in a final death of bacteria; the therapeutic effect of the acne therapeutic agent is comparatively excellent after being repeatedly tested.
EP1129112B1 Peptides containing a cholesterol recognition sequence and their uses A cholesterol interaction/recognition consensus sequence is described and methods of use thereof.
EP2655323A1 Ingenol-3-acylates iii and ingenol-3-carbamates The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is -NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
CN101066459B Polyesthylene glycol modified zidovudine conjugate and its preparation process and application The present invention relates to one kind of polyethylene glycol modified zidovudine conjugate and its preparation process and application. The polyethylene glycol modified zidovudine conjugate with the structure as shown is prepared through dissolving zidovudine, p-dimethyl aminopyridine and dicyclohexyl carbon diimide in proper amount of dichloromethane, dropping equi-molar ratio dichloromethanesolution of mPEG-SA to react, filtering, adding cold ether in 45-55 times volume into the filtrate to obtain white precipitate, filtering to separate the precipitate, and drying to obtain precursor methoxy polyethylene glycol zidovudine conjugate for preparing anti-AIDS medicine.
CA2260774C Substituted triazolo-pyridazine derivatives as ligands for gaba receptors A class of substituted or 7,8-ring fused 1,2,4triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA A receptors, in particular having high affinity for the a2 and/or 0 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
CN102085236A Oral liquid for helping reduce blood fat The invention relates to oral liquid for helping reduce blood fat and particularly provides the oral liquid for safely and effectively helping reduce blood fat. The oral liquid is prepared from the following active ingredients and auxiliary materials in part by weight: 250 to 300 parts of active ingredients and 700 to 800 parts of purified water, wherein the active ingredients are prepared from the following raw materials in part by weight: 100 to 150 parts of levo-carnitine and 500 to 600 parts of kudzuvine root. The oral liquid has the synergistic action of reducing blood fat and simultaneously does not generate any acute or subacute hazards.
CN102000026A Naproxen orally-taken micro-emulsion preparation and preparation method thereof The invention relates to an orally-taken micro-emulsion preparation and a preparation method thereof, in particular a naproxen orally-taken micro-emulsion preparation and a preparation method thereof, belonging to the technical field of medicines. The orally-taken micro-emulsion preparation uses naproxen as the main pharmacological ingredient and contains medicinal oil, emulsifier, assistant emulsifier and water for injection. The naproxen orally-taken micro-emulsion preparation is orally administrated and has clear appearance; the grain diameter evenly ranges within 10nm-100nm; all phase are of the same property and have thermodynamic stability; the medicine loading rate ranges from 0.0%-3.5%; the preparation process is simple; and the quality is stable and can be easily controlled. The naproxen prepared into the orally-taken micro-emulsion preparation can be absorbed through lymphatic vessels as a result of lower surface tension of the micro-emulsion, therefore, the first-pass effect of the liver and obstacles for macromolecule to pass through the gastrointestinal tract epithele cell membranes can be overcome.
US20120142648 Methods for delivering clonidine compositions in biodegradable polymer carrier and local steriods to a target tissue site Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine and a steroid at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.
US20070248639 Cyclooxygenase inhibitor and calcium channel antagonist compositions and methods for use in urological procedures Compositions of a cyclooxygenase inhibitor and a calcium channel antagonist in a liquid carrier. The composition may be administered the the urinary tract during urological diagnostic, interventional, surgical and other medical procedures. One disclosed composition comprises ketoprofen and nifedipine in a liquid irrigation carrier, and includes a solubilizing agent, stabilizing agents and a buffering agent.
CN101773495A Anti-tumor medicinal composition and application and preparation method thereof The invention relates to an anti-tumor medicinal composition consisting of an effective dose of active ingredient compound SHC-10 which is used for treating tumor diseases and is extracted from plant cephalotaxus lanceolata and a medicinal carrier, a preparation method thereof and application of the compound SHC-10 and the medicinal composition thereof in preparing a medicament for restraining the tumor diseases, particularly the medicament for resisting gastric cancer, liver cancer and breast cancer.
US20120264999 4 (pyrrolopyridinyl)pyrimidin-2-ylamine derivatives Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in claim 1, are inhibitors of cell proliferation/|cell vitality and can be employed for the treatment of tumours
WO2008006563A1 Purine derivatives as a2a agonists Compounds of formula (I):or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R1,R 2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
US20110160252 Pharmaceutical compositions for treatment or prevention of hbv infection First, the present inventors assessed the effect of the compound represented by formula (III) below on Huh-7 cells infected with HBV, and demonstrated that the compound alone had an anti-HBV effect in vitro. Formula (III) Then, the present inventors revealed that the HBV replication-suppressing effect of PEG-IFN is enhanced in chimeric mice having a human liver infected with genotype C or A HBV when PEG-IFN is used in combination with the compound represented by formula (III) above. The present inventors also revealed that the HBV replication-suppressing effect of Entecavir is enhanced in chimeric mice having a human liver infected with genotype C HBV (wild-type and Entecavir-resistant strains) when Entecavir is used in combination with the compound represented by formula (III) above. In addition, the present inventors revealed that the compound represented by formula (III) above exerts the anti-HBV effect not only against wild-type HBV strains but also against Entecavir- and/or Lamivudine-resistant HBV strains.
EP1221985B1 Conveyance of anti-infective activity to wound dressings A wound dressing having anti-infective activity. The wound dressing provides stable and improved formulations of precursors required in generating anti-infective iodine specifically within a wound site where the oxygen tension may be very low. Furthermore, the design of the invention precludes interference by catalase (and other heme proteins) in competing for hydrogen peroxide where hydrogen peroxide is used as a component of the iodine generating formulation, ensuring more efficient and sustained production of free iodine as a potent anti-infective agent. The invention takes advantage of the physical design of the wound dressing, and the permeation of the body fluid into the dressing, which together serve to initiate formation of nascent iodine concomitant with placement of the dressing into, or over, a wound site. The invention circumvents the problem of trapping elemental iodine in the form of tri-iodide, which lacks microbicidal activity, by the chemical method of generating iodine de novo, and in the presence of excess oxidant. Newly formed iodine is thus able to egress and disperse throughout the wound site before there is an opportunity for it to become fully bound as tri-iodide, conferring to the wound site anti-infective activity. Two embodiments of the wound dressing invention are described comprising a mono- and bilayer configuration which, when placed in a wound site, confer to the site anti-infective properties.
US20120083500 Oxazolone and pyrrolidinone-substituted arylamides as p2x3 and p2x 2/3 antagonists Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
CA2806619A1 Anti-diabetic compositions and methods The present invention is concerned with synergistic compositions effective in the treatment of diabetes. In particular, the present invention is concerned with synergistic compositions comprising inulin, or a suitable source thereof, and Sulphonylureas used in the treatment of type-2 Diabetes Mellitus (T2DM) and hyperglyacemia.
WO2011152071A1 Novel hyaluronic acid decomposition-promoting factor and inhibitor thereof Disclosed is a novel factor KIAA1199 that participates in the decomposition of hyaluronic acid, and also disclosed is the use thereof. Specifically disclosed are: a hyaluronic acid decomposition promoter comprising the KIAA1199 gene and protein thereof; a hyaluronic acid decomposition inhibitor (comprising siRNA or monoclonal antibody) that inhibits the activity or expression of the hyaluronic acid decomposition promoter; and a method for screening for a novel hyaluronic acid decomposition inhibitor using KIAA1199 expression as the indicator.
US20080188472 Indole-2-Carboxylic Acid Hydrazides Compounds of formula (I) or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia, e.g. myocardial ischemia, or as cardioprotectants or inhibitors of abnormal cell growth.
CN1788792A Pharmaceutical combination for preventing and treating fallopian tube adhesion The present invention belongs to the field of medicine technology, and is one medicine composition for preventing and treating oviduct adhesion. The medicine composition has the main components including sodium hyaluronate, antibiotics and glucocorticoid. The present invention features the sodium hyaluronate as physical rack with excellent adhesion preventing effect, and antibiotics and glucocorticoid with antiphlogisic and analgetic effect to make the medicine composition possess the integral adhesion preventing, antiphlogisic and analgetic effects to prevent and treat oviduct adhesion effectively. In addition, sodium hyaluronate with the functions of increasing viscosity, biological adhesion, spreading, moistening and delayed releasing can increase the absorption of antibiotics and glucocorticoid, reduce the toxic side effect caused by systemic absorption and decrease negative reaction.
US20100330097 Predicting amd with snps within or near c2, factor b, plekha1, htra1, prelp, or loc387715 Gene polymorphisms and genetic profiles associated with an elevated or a reduced risk of a complement cascade dysregulation disease such as AMD are disclosed. Methods and reagents for determination of risk, diagnosis and treatment of such diseases are provided, as well as methods and reagents for determining sequence variants in the genome of an individual which facilitate assessment of risk for developing such diseases are provided.
US7320784 Metal support surface, conjugate releasably bound to the support surface, the conjugate comprising a ligand and a targeting molecule;wherein the conjugate coordinates with a complex-forming metal ion so that labeled conjugate is released; radiotherapy and as imaging agents in medical diagnostics The invention includes methods and compounds for labelling conjugates with metals which comprise the steps of coupling the conjugate to a support surface; introducing a complex-forming metal to the support; and collecting the metal-conjugate complex released from the support. The metal catalyzes cleavage of the conjugate from the support upon complex formation resulting in a solutions substantially free of unlabeled conjugate.
WO2008080971A1 Substituted oxindole derivative and its use as a vasopressin receptor ligand The present invention relates to novel oxindole derivatives of the formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.
CN1622754A Novel immune effect compound This invention provides compounds containing a 2-deoxy-2-amino- beta -D-glucopyranose (glucosamine) glycosidically linked to an cyclic aminoalkyl (aglycon) group. The invention further provides methods for inducing an immune response using the compounds of the present invention in the presence or absence of an antigen. In addition, methods for treating disease with the compounds of the present invention with or without an antigen are also provided in this invention.
US20080076725 less hygroscopic The present invention relates to a clathrate of azithromycin hydrate with 1,2-propyleneglycol of formula (I), a method for the manufacture thereof, and a pharmaceutical composition containing same. The inventive compound is much less hygroscopic than azithromycin hydrate or crystals known in the art, therefore, it can be useful for the preparation of a medicine for treating various microbial infections. wherein m ranges from 1 to 2 and n, from 0.30 to 0.45.
CN101703490A Polysaccharide/inorganic nanoparticles hybrid micron-nano medicine-carrying capsule The invention discloses polysaccharide/inorganic nanoparticles hybrid micron-nano medicine-carrying capsule. The capsule has the following structure characteristics: (1) a water in oil (W/O) microemulsion capsule core is prepared by using fat-soluble drug A or fat-soluble drug B which is dissolved in oily solvent, negative OSA modified polysaccharide derivative and water; (2) the polysaccharide and negative inorganic nanoparticles perform layer-by-layer self-assembly which is based on the electrostatic interaction to form a capsule wall; and (3) the grain size of the micron-nano medicine-carrying capsule is 50-1000nm. The micron-nano medicine-carrying capsule provided by the invention has high drug encapsulation efficiency for drug situ embedding, the raw materials are all adopted from biodegradable materials with good biocompatibility and biodegradability. In addition, the medicine-carrying system has double intelligent functions of targeting and controlled release.
US7144897 Substituted amide compound containing hydroxy and amino groups; useful for treating Alzheimer's disease and other similar diseases Disclosed are compounds of formula X, which are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.
EP1322590B1 5-amino-1-pentene-3-ol substituted derivatives The invention relates to 5-amino-1-pentene-3-ol substituted derivatives, a method for the production thereof, medicaments containing said compounds and the use of substituted 5-amino-1-pentene-3-ol derivatives for the production of medicaments.
US20110086049 Receptor Modulators Method of identifying a modulator of CD28 comprising comparing a structural model of a candidate modulator with a structural model of CD28 to thereby determine whether the modulator will bind to CD28, wherein the structural model is derived from, or comprises, structural coordinates of a crystal of: (i) CD28, (ii) a fragment of CD28, or (iii) a homologue of (i) or (ii). The crystal of CD28 in a soluble form complexed with the Fab fragment of a mitogenic (superagonistic) antibody has been obtained and used for the determination of the 3D-structure of the receptor. The application also relates to modulators of superagonistic signalling for any receptor of the CD28 family, i.e. to superagonistic antibodies and chimeric proteins thereof, and to the screening of the superagonistic modulators. In the methods of screening, the binding of the candidate modulators to a portion of the receptor proximal to the cell membrane is investigated.
WO2006062224A1 Carboxamide derivative An SGLT inhibitor comprising a compound of the formula: (|) wherein the ring A is an optionally substituted ring; R1 is an optionally substituted hydrocarbon group, etc.; each of R2 and R3 independently is a hydrogen atom, an optionally substituted hydrocarbon group, etc.; R4 is an optionally substituted hydrocarbon group, etc.; and X is a bivalent chain group whose main chain consists of 1 to 6 atoms. This SGLT inhibitor is useful as a preventive/therapeutic agent for diabetes mellitus, obesity, hypertension, hyperlipemia, etc.
EP1140026B1 Biodegradble polymer encapsulated serotonin receptor antagonist and method for preparing the same A new class of biodegradable pharmaceutical compositions useful as sustained release medicamentous compositions, including methods of making and methods of using these compositions, are described and claimed. The method of making these compositions includes the steps of: a) dry mixing of a pharmaceutically active molecule with a biodegradable polymer; b) melt extruding the mixture to form a solid solution of the active molecule in the polymer; and c) pulverizing the solid solution to form microparticles such that they can be formed into injectable formulations. Preferred embodiments include pharmaceutical compositions of polylactide-co-glycolide and (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ehtyl]-4-piperidinemethanol (active ingredient) and a method for its formation. These compositions release the active ingredient at a steady rate over a period of days to weeks. The active ingredient antagonizes the effects of serotonin at the 5HT2A receptor and are useful in treating various conditions such as, for example, psychoses including schizophrenia, obsessive compulsive disorder, sleep disorder, depression, anorexia, anxiety, drug addiction and bipolar disorders.
WO2006105850A8 Acyl hydrazides as kinase inhibitors, in particular for sgk Novel acyl hydrazides of the formula (I), in which R1 - R9 have the meanings defined in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions such as diabetes, obesity, metabolic syndrome (dyslipidemia), systemic and pulmonary hypertension, cardiovascular diseases and kidney diseases, and generally any types of fibroses and inflammatory processes.
US20090186886 Tricyclic 1,2,4-Triazine Oxides and Compositions for Therapeutic Use in Cancer Treatments The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula I and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
US20080025945 treating hepatic fibrosis; liver cirrhosis; administering to a patient an effective low dose of IL-6, a mutein, fused protein, active fraction or circularly permutated derivative The invention relates to the use of IL-6 in liver cirrhosis.
EP0750507B2 Proteasome regulation of nf-kappa-b activity Disclosed herein is a method for regulating the activity of NF-λB in an animal comprising contacting cells of the animal with certain proteasome inhibitors.
WO2008037888A3 Tetracyclic compounds, process for the preparation thereof pharmaceutical compositions comprising the same and use thereof as dopaminergic receptor ligands Compounds of formula (I), of trans relative configuration: in which: X is an oxygen atom or an NR2 group, Y is a group selected from -CH2-, -(CH2)2- and -CH=CH-, R1 and R2, which may be identical or different, are each a hydrogen atom or a group selected from alkyl, cycloalkyl and cycloalkylalkyl, in racemic form or in the form of optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof. Said compounds are useful as dopaminergic receptor ligands for the treatment of central nervous system diseases.
US20100119623 Imidazolyl modulators of 5-ht3 receptors The present invention relates to new imidazolyl modulators of 5-HT3 receptors, pharmaceutical compositions thereof, and methods of use thereof.
WO2008113359A2 1- [2-(2,4-dimethylphenylsulfanyl)-phenyl] piperazine as a compound with combined serotonin reuptake, 5-ht3 and 5-ht1a activity for the treatment of pain or residual symptoms in depression relating to sleep and cognition The use of l-[2-(2,4-dimethylphcnylsulfanyl)phcnyl]piperazine in the treatment of pain and residual symptoms in depression is provided.
CN101396364A Zaleplon oral-cavity administration system or composition and preparation method thereof The invention relates to a zaleplon oral administration preparation which belongs to the pharmacy field. The zaleplon oral administration preparation consists of active component zaleplon and medically acceptable auxiliary material. Every 100ml of the preparation contains 1 to 10g of zaleplon. The zaleplon oral administration preparation has the advantages that the zaleplon is preferred as the active component in a sublingual administration system; the system or combination feeds drugs by a spray form; the zaleplon oral administration preparation can avoid gastral action and liver first-pass effect and has the advantages of fast effect, high bioavailability, exact curative effect, convenient usage, adjustable dose according to the requirement and good adaptability; the zaleplon oral administration preparation is particularly fit for the elderly and the patient inconvenient for swallowing; the zaleplon oral administration preparation has the advantages of simple and feasible preparation technology and fit for the industrialized production, etc.
WO2008154563A1 1, 3 - dihydroxy substituted phenylamide glucokinase activators Compounds are provided which are glucokinase activators and thus are useful in treating diabetes and related diseases and have the structure wherein in the ring represents one or two double bonds; R1 is alkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; R2 is alkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; R5 is as defined herein; Z is O, S, S(O), S(O)2, or NR5a; X is S, O, N, NR3, or CR3; Y is NCR4 or NR4; R3, R4, and R5 are as defined herein; R8 is aryl, heteroaryl, -PO(OR9)(OR10), -PO(OR9)R10 or -P(O)(R9)R10 (wherein R9 and R10 are as defined herein)/ R6 and R7 are independently H, halogen, or alkyl; m is 0 or 1; and n is 0 to 3, or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
CN102846769A Preparation process of integration-type novel formulation of Semen Persicae Chengqi decoction and production method thereof The invention relates to a preparation process of integration-type novel formulation of Semen Persicae Chengqi decoction and a production method thereof. The effective components of the novel formulation are made from the following raw materials (by weight parts): Semen Persicae (Prunus persica and/or Prunus davidiana) 12, Radix Et Rhizoma Rhei 12, Cinnamomum cassia twig 6, mirabilite 6 and Radix Glycyrrhizae 6. The production method includes the steps of supersonic airstream pulverization, alcohol-water extraction, ultrasonic pulverization and extraction, water decoction and concentration, supersonic spray-drying, nano-scale grinding, high-pressure emulsion and homogenization and nanoparticle preparation. The production method integrates the advantageous of the nano-carrier combination technique, such as multi-component synergism and multi-target. The large-scale production can greatly reduce the production cost, greatly improve the product quality and enhance the target property and sustained/controlled-release property of drugs. The novel formulation is administered by oral intake and external application during four time periods respectively based on the midnight-noon tidal flow and human qi-blood flow rule. The novel formulation is also processed to membranes and transdermal delivery agents which are applied to different parts of human body respectively according to the midnight-noon tidal flow and human qi-blood flow rule and can be directly absorbed by the skin.
EP1499608A1 Substituted imidazole derivatives: gaba a receptor ligands Substituted imidazole derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies). (Formula I)
CN1864664A Lmiquimod cream and preparation method thereof The present invention relates to imiquimod cream containing imiquimod of grain size not greater than 100 micron in 1.0-10.0 wt%, oil phase, water and emulsifier. The preparation process of imiquimod cream includes the following steps: heating at 75-85 deg.c to smelt oil phase with added thickener and anodyne; mixing humectant and water to obtain water phase and heating to 75-85 deg.c; mixing imiquimod, emulsifier, preservative, oil phase and water phase via maintaining the temperature and stirring for 15-20 min; and regulating pH value to 4.0-7.0 to obtain the imiquimod cream. The medicine of the present invention has raised permeating absorption and raised curative effect, and is used in treating condyloma acuminatum around male's and female's external genitalia and anus.
CN101875680A Nucleoside compound, preparation method and application thereof The invention discloses a 5'-desoxy-5-flucytosine L-ribose nucleoside compound and a medicinal salt thereof. The general formula of the chemical structure of the compound is shown as a formula (L), wherein R1 is hydrogen, straight-chain or branched alkyl containing 1 to 6 carbon atoms, substituted or unsubstituted aryl or low-level aralkyl, the aryl is substituted or unsubstituted monocyclic or dicyclic compound containing at least one aromatic ring, and the low level aralkyl is low-level alkyl connected with the aryl; and R2 is a straight-chain or branched alkyl containing 1 to 6 carbon atoms, substituted or unsubstituted aryl or low-level aralkyl, the aryl is substituted or unsubstituted monocyclic or dicyclic compound containing at least one aromatic ring, and the low level aralkyl is low-level alkyl connected with the aryl. The invention also discloses a preparation method and application of the compound. The 5'-desoxy-5-flucytosine L-ribose nucleoside compound (L) has strong activity of tumor resistance and virus resistance, and the preparation method has lower cost and high yield.
US20060270640 Method of preventing, medicating, and/or treating hypocalcemia of domestic mammal The present invention provides a method of preventing, curing, and/or treating hypocalcemia of a domestic mammal, especially, a cow. Specifically, the present invention provides a method of administrating a vitamin D derivative to prevent, cure and/or treat hypocalcemia, characterized in that a vitamin D derivative, especially, 1α-hydroxyvitamin D3 and/or 1.25-dihydroxyvitamin D3 is transvaginally administered to a domestic mammal.
WO2014095920A1 New cyclohexyl and quinuclidinyl carbamate derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activity The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
CN103446061A Developing nano-silver sodium alginate microsphere vascular embolizing agent and preparation method thereof The invention discloses a developing nano-silver sodium alginate microsphere vascular embolizing agent and a preparation method of the vascular embolizing agent, relates to a vascular embolizing agent and a preparation method of the vascular embolizing agent, and aims at solving the technical problems that the existing developing embolizing agent is short in developing time and has potential biological toxicity. The developing nano-silver sodium alginate microsphere vascular embolizing agent comprises a carrier and a developing substance. The preparation method comprises the following steps of dropwise adding a sodium alginate solution containing a nano-silver particle into a calcium chloride solution prepared in the step 5 to obtain the developing nano-silver sodium alginate microsphere vascular embolizing agent. The developing medicine-loaded nano-silver sodium alginate microsphere vascular embolizing agent disclosed by the invention is good in visibility under X ray, the embolizing degree can be conveniently observed, and the mistaken embolizing can be effectively prevented; the vascular embolizing agent has biodegradation performance and can be degraded to nontoxic and harmless substances to be eliminated from the body after the embolizing; the vascular embolizing agent has biocompatibility and can prevent the other injuries on organs; the diameter of the micro-particle can be controlled; and the medicine release rate can be controlled.
CN101134031A Use of arctigenin in the preparation of medicament for treating and preventing chronic renal failure and kidney fibrosis The present invention is use of arctigenin in preparing medicine for preventing and treating chronic kidney failure and kidney fibrosis. The present invention also provides medicine composition with arctigenin as active component for preventing and treating chronic kidney failure and kidney fibrosis. When the medicine composition is applied in preventing and treating chronic kidney failure and kidney fibrosis, the injection has dosage of 30mg-1000 mg, preferably 30-500 mg, and the orally taken dosage is 50-2000 mg, preferably 50-800 mg.
US20120244214 Methods for treating multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)-piperidine-2,6-dione in combination with proteasome inhibitor Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
WO2007093587A1 Use of r-(-)-2,4-diamino-5-(2, 3-dichlorophenyl)-6-fluoromethyl pyrimidine for the treatment of psychotic disorders The present invention is concerned with the use of R(-)-2,4-diamino-5-(2,3-dichlorophenyl)-6-fluoromethyl pyrimidine of formula (I), or pharmaceutically acceptable salts, solvates or prodrugs thereof, either as monotherapy or in combination with another therapeutic agent, for the treatment of psychotic disorders:
CN102138931A Application of selenium serving as trace element necessary for human bodies to preparation of externally-applied medicaments for onychomycosis and tinea unguium The invention relates to application of selenium serving as a trace element necessary for human bodies to the preparation of externally-applied medicaments for onychomycosis and tinea unguium. Antifungal ingredients of the medicaments are prepared by blending the selenium serving as the trace element necessary for the human bodies and liquid solvent and grease auxiliary materials. The medicaments have the characteristics of high curative effect, short treatment course, low cost and the like, and a treatment method is simple and convenient.
US20130022641 Anti-Tumor Agent and Immunostimulating Agent To provide a pharmaceutical composition comprising a ceramide-related substance having little adverse side effects as an active ingredient by using a raw material that is highly safe to a human body and is inexpensive. A pharmaceutical composition comprising at least one sphingoglycolipid derivative that is produced from a beer waste and is represented by the formula below as an active ingredient: wherein R3 represents H or OH; R4 is as defined by (a) or (b) (a) when R3 is H, R4 represents (CH2)13CH3 or (CH2)6CH═CHCH2CH═CH(CH2)4CH3; and (b) when R3 is OH, R4 represents (CH2)yCH3 (where Y represents an integer of 13 to 21) or (CH2)Z1CH═CH(CH2)Z2CH3 (where Z1 and Z2 independently represent 0 or a natural number, provided that Z1+Z2=19).
WO2006073042A1 ACTIVATOR FOR Nrf2-DEPENDENT GENE [PROBLEMS] To provide a transfer activator for Nrf2-dependent genes which is usable in foods, cosmetics, medicines, quasi-drug preparations, etc. [MEANS FOR SOLVING PROBLEMS] The transfer activator is for genes dependent on transfer factor Nrf2 and is characterized by containing a shogaol compound represented by the following general formula [A]. [In the formula [A], R1 to R5 each independently represents hydrogen, lower alkyl, hydroxy, lower alkoxy, or C1-15 acyloxy; R6 represents hydrogen, hydroxy, lower alkoxy, C1-15 acyloxy, carboxy, or COOR7 (R7 represents C1-8 linear or branched alkyl); and n is an integer of 1-20.]
CN103083332A Application of tanshinone IIA to preparing drugs or cosmetics for inhibiting propionibacterium acnes The invention discloses an application of tanshinone IIA in preparing drugs or cosmetics for preventing or treating comedo caused by reproduction of propionibacterium acnes. The tanshinone IIA is capable of effectively treating the acnes caused by the reproduction of the propionibacterium acnes. The tanshinone IIA is obtained from dry roots or rhizomes of Salvia miltiorrhiza Bge, has low toxicity to human bodies and has a high inhibition effect on the propionibacterium acnes; and therefore, the tanshinone IIA can be prepared into various drug forms for external use and cosmetics, and has an excellent application prospect.
CA2547355A1 Animal models of pancreatic adenocarcinoma and uses therefor The present invention is based, at least in part, on the generation of an animal model of pancreatic adenocarcinoma which recapitulates the genetic and histological features of human pancreatic adenocarcinoma, including the initiation, maintenance, and progression of the disease. Accordingly, the present invention provides animal models of cancer, e.g., pancreatic adenocarcinoma, wherein an activating mutation of Kras has been introduced, and any one or more known or unknown tumor suppressor genes or loci, e.g., Ink4a/Arf, Ink4a, Arf, p53, Smad4/Dpc, Lkb1, Brca2, or Mlh1, have been misexpressed, e.g., have been misexpressed leading to decreased expression or non-expression. The animal models of the invention may be used, for example, to identify biomarkers of pancreatic cancer, to identify agents for the treatment or prevention of pancreatic cancer, and to evaluate the effectiveness of potential therapeutic agents.
US20100222353 Aminophthalazine derivative compounds The invention pertains to new aminophthalazine compounds that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds that are selective inhibitors of PDE-10. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom.
WO2007029078A3 Succinimide and glutarimide derivatives as adrenergic receptor antagonists The present invention relates to succinimide and glutarimide derivatives having the structure of Formula I, which can be used to treat a disease or disorder mediated through α1a and/or α1d adrenergic receptors. Compounds and pharmaceutical compositions disclosed herein can be used to treat benign prostatic hyperplasia (BPH) and related symptoms thereof. Further, such compounds can be used to treat lower urinary tract symptoms that may or may not be associated with BPH. The present invention also relates to processes to prepare the disclosed compounds, pharmaceutical compositions thereof, and methods of treating BPH or related symptoms thereof.
CN101906090A 3,4-dihydro-4-aryl coumarin compounds as well as preparation method and application thereof The invention discloses 3,4-dihydro-4-aryl coumarin derivatives as well as a preparation method and application thereof. The preparation method comprises the following steps of: with substituted benzaldehyde and malonic acid as raw materials, heating in the presence of pyridine and piperidine and generating a Perkin reaction and a decarboxylic reaction to obtain substituted phenylacrylic acid derivatives; and then subjecting the substituted phenylacrylic acid derivatives and phenol compounds to a reaction in the presence of the catalysis of boron trifluoride diethyl ether and phosphorus oxychloride to obtain the 3,4-dihydro-4-aryl coumarin compounds. The compounds can be used for preparing medicaments for resisting tumors, abnormal vascular proliferation, bacterial and oxidation.
CN101507711A Ligustrazine micro-spheres and preparation method thereof The invention discloses a ligustrazine microsphere. A carrier of the ligustrazine microsphere is a poly lactic acid-glycollic acid copolymer, and a slow-release drug is ligustrazine, wherein the content of the ligustrazine accounts for 8.82 to 9.51 percent of the mass of the total microsphere. The invention also discloses a method for preparing the ligustrazine microsphere. The method comprises that: the ligustrazine and the poly lactic acid-glycollic acid copolymer are dissolved in methylene chloride to form an oil phase, the oil phase is slowly added in a water phase(a gelatine solution or solution of polyvinyl alcohol) dropwise at a constant speed and cut at a high speed to obtain an O/W emulsion; the O/W emulsion is dispersed in the water phase and stirred for 1 to 3 hours, so that the organic solvent of methylene chloride is completely volatilized; and an upper layer liquid is removed by centrifugation, and the obtained product is washed by distilled water for 3 to 5 times and vacuum-dried for 12 to 80 hours to obtain the dry powder of the ligustrazine microsphere. The ligustrazine microsphere can act on arthritis of a knee bone in high selectivity, the effect is strong and durative, no toxic and side effect exists, and the defect of long-time and frequent drug administration is avoided; and when used to treat the arthritis, the ligustrazine microsphere can achieve good effects.
CN102836304A Plaster used for treating bone spurs The invention discloses a plaster used for treating bone spurs. The plaster is characterized by that the plaster is prepared from the raw materials of, by weight: 10-15 parts of common achyranthes, 10-15 parts of cassiabarktree twig, 10-15 parts of Manchurian wildginger herb, 8-10 parts of eucommia, 8-10 parts of dragon's blood, 10-15 parts of myrrh, 15-20 parts of pangolin scales, 10-15 parts of loofah sponge, 10-15 parts of Chinese clematis root and rhizome, 8-10 parts of borneol, 15-20 parts of kadsura pepper twig and leaf, 15-20 parts of incised notopterygium rhizome and root, 15-20 parts of doubleteeth angelica root, 10-15 parts of largeleaf gentian root, 10-15 parts of common monkshood mother-root, and 15-20 parts of jackinthepulpit tuber. The plaster provided by the invention has various functions of blood circulation activating, qi regulating, stasis dissipating, pain relieving, evil dissipating, body resistance supporting, and the like. The treatment effect of the plaster is good, and a curative speed is high.
WO2010026760A1 Compositions wherein bioactive components are stably sealed Provided are compositions, wherein compounds that are easily oxidized are stably sealed in a base material without using conventional antioxidants and excipients. Provided are compositions that comprise biopolymers, biodegradable synthetic polymers, and bioactive components.
CA2149408C Compositions for curing affected abnormal tissues, method for the preparation thereof, and usage thereof Injectable preparations of the composition for curing affected abnormal tissues are prepared by formulating sodium hydrogen sulfite with all the other components except tannic acid to yield a first mixture and adding tannic acid to the first mixture or by formulating a water-soluble aluminum compound and a chelating agent to yield a first formulation, formulating tannic acid and sodium hydrogen sulfite to yield a second formulation and admixing the first formulation with the second formulation to yield a second mixture and, as needed, adding a poly-valent alcohol and/or a saccharide to the first and/or second formulations or to the first or second mixture. This preparation can prevent tannic from being oxidized and from reacting directly with an aluminum ion derived from sodium hydrogen sulfite, whereby the composition having a stable formulation can be provided. The resulting compositions for curing the affected abnormal tissues is stable in quality and constant in formulation.
WO2006116470A1 Use of metformin to counteract weight gain associated with aripiprazole or ziprasidone treatment A method for minimizing the weight gain side effect associated with ABILIFY® (aripiprazole) or GEODON® (ziprasidone) treatment is disclosed. In this method, metformin, a biguanide compound, is concurrently administered to a patient taking the ABILIFY® (aripiprazole) or GEODON® (ziprasidone) therapy. A pharmaceutical composition containing the combination of ABILIFY® (aripiprazole) or GEODON® (ziprasidone), together with metformin is also disclosed.
CN101130566A Method of preparing 23,24-dihydrocucurbitacin B and use of the same in medicament for treating tumour The invention discloses a preparing method of 23,24-dihydrocucurbitacin B and usage to treat tumor disease medicine, which comprises the following steps: using adverse current chromatogram; proceeding primary separation for acetic acid ethyl ester extract of trichosanthes anguina root; choosing two phase dissolvent system from light petroleum, chloroform and acetonitrile; merging and collecting the compound with cell toxic property; proceeding against phase high effective liquid phase color spectrum preparation with flowing phase as methanol and water gradient elution; collecting goal matter; volatilizing dissolvent; getting white crystalline powder; getting the product. This invention can be used to prepare the medicine of breast cancer, liver cancer and large intestine cancer, which possesses wide prospect.
CN103641764A Pharmaceutical composition for regulating blood lipid The invention relates to a pharmaceutical composition for regulating blood lipid. Specifically, the invention relates to a bulk pharmaceutical chemical, which comprises an active ingredient shown as a formula I or a hydrate thereof such as a trihydrate. Further, the invention also relates to a pharmaceutical composition, which contains the bulk pharmaceutical chemical and optionally pharmaceutically acceptable carriers or excipients. The bulk pharmaceutical chemical or pharmaceutical composition thereof provided by the invention can be used as a hypolipemic drug for clinical application to the treatment or prevention of hypercholesterolemia and coronary heart disease.
WO2011121453A3 Methods and compositions for treating or ameliorating cancer using gemcitabine-5'-elaidate This invention provides methods and compositions for treating or otherwise ameliorating cancer in a subject, along with methods and compositions for measuring the levels of nucleoside transporters in a tumor and correlating this level to a predicated efficacy of a given anti-cancer drug regime, and methods and compositions for treating patients with low levels of hENTI expression in cancer cells using a lipophilic gemcitabine analog such as gemcitabine-5'-elaidate.
WO2013108026A1 Thiadiazolone derivatives useful in the treatment of diabetes According to the invention there is provided a compound of formula I, wherein, R1 to R4 have meanings given in the description, which compounds are useful in the treatment of diabetes.
WO2007070984A1 Spiroketals The present invention relates to spiroketal compounds that are useful in methods of treating or preventing protozoal infections, parasitic infections, bacterial infections, cell proliferative disorders and anti inflammatory disorders. The spiroketal compounds are also useful as immunosuppressive agents, and also in methods of controlling pests.
EP2079731A1 Novel substituted piperidyl-propane-thiols One object of the present invention are novel substituted piperidyl-propane-thiols of the formula (1), wherein R1, R2, R3 and D are defined as below. Another object of the present invention is to provide agonists or antagonists of CCR-3, or pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
US20100278931 Porous silicon drug-eluting particles The invention provides a biodegradable drug-eluting particle useful for the delivery of diagnostic or therapeutic agents. In certain embodiments, the drug-eluting particle of the invention comprises a biodegradable porous silicon body, a reservoir formed within the porous silicon body having at least one opening to an exterior of the body, wherein the reservoir contains a therapeutic or diagnostic agent, and an agent-permeable seal disposed over the at least one opening. The invention further provides a method for treating a patient to obtain a desired local or systemic physiological or pharmacological effect comprising administering a sustained release drug delivery particle of the invention. The invention also provides methods of fabricating a drug-eluting particle for releasing therapeutic agents
CN1931229A Medicine for treating acute and chronic nasopharyngitis and its prepn process The present invention discloses one kind of me for treating acute and chronic nasopharyngitis. The medicine is prepared through mixing patchouli oil in 1-30 weight portions and hyodesoxycholic acid in 10-300 weight portions, adding proper amount of supplementary material for orally taken preparation and re-mixing. The medicine of the present invention is used in treating nasopharyngitis and has the outstanding advantages of small dosage, easy taking, high effect and fast acting.
US20090252706 Tetrahydropyridothiophenes As Antripoliferative Agents For The Treatment Of Cancer The invention relates to compounds of formula (I) wherein Ra is —C(O)ORI, in which R1 is 1-7C-alkyl. 3-7C-cycloakyl, 1-7C-alkyl substituted by Raa, or 2-7C-alkyl substituted by Rab and Rac on different carbon atoms, Rb is -T-Q, in which T is 1-6C-alkylene or 3-7C-cycloalkylene, and Q is substituted by Rba and Rbb and Rbc, and is phenyl, which are useful for the therapy of hyperproliferative diseases, in particular human cancer.
WO2011032229A1 A novel epsilon polymorphic form of inulin and compositions comprising same A novel polymorphic form of inulin, designated epsilon inulin (eIN), is described along with methods for the preparation of eIN, compositions comprising eIN and uses thereof. Amongst the uses described is the stimulation of an immune response in a subject for the purposes of preventing or treating an infectious disease, autoimmune disease, immunodeficiency disorder, neoplastic disease, degenerative or ageing disease.
US20080182896 Use of metal chelates in human or animal feeding The present invention relates to the use in human and animal nutrition (monogastric and polygastric animals) of known chelates of bivalent metal Mg, Ca, Mn, Co, Cu, Zn and Fe with methionine hydroxy analogue. The present invention further relates to a method for preparing new chelates with methionine hydroxy analogue, both in solid form with iron (II), vanadium (iV) and (V) and molybdenum (V) and (VI), and in liquid form in aqueous solution with iron (II) and (III) and chrome (III). Eventually, the present invention relates to the use of said new chelates, both in solid form with iron (II), vanadium (IV) and (V) and molybdenum (V) and (VI), and in liquid form in aqueous solution with iron (II) and (III) and chrome (III), in human and animal nutrition.
EP1731169A1 Remedies for prostatic hypertrophy A treatment and/or preventive agent for prostatic hypertrophy includes a compound having an antagonistic effect to an angiotensin II receptor, or a pharmaceutically acceptable salt or a prodrug thereof, as an active ingredient, wherein said compound having an antagonistic effect to an angiotensin II receptor is one or more compounds selected from the group consisting of losartan, potassium losartan, candesartan, candesartan cilexetil, balsartan, eprosartan, zolasartan, telmisartan, irbesartan, tasosartan, olmesartan medoxomil, and olmesartan.
US7122565 Thiadiazoles and oxadiazoles and their use as phosphodiesterase-7 inhibitors The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following Formula I: in which, Y is S or O, R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, optionally substituted, R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl or aryl optionally substituted, R3 is X2—R′3, in which X2 is a binding group and R′3 is cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl, or a polycyclic group; optionally substituted, or their pharmaceutically acceptable derivatives, a compound of Formula I, for their preparation, and processes for pharmaceutical compositions containing methods of using the compounds for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.
US20100303803 Catenate for immunostimulation The invention relates to a multimeric, non-coding nucleic acid molecule for modulating the activity of the human or animal immune system, and to a production method therefor, and to a vaccine containing said multimeric, non-coding nucleic acid molecule. Said multimeric, non-coding nucleic acid molecules can be non-coding nucleic acid molecules that consist of at least two of said molecules (dimer) or assemblies of several non-coding nucleic acid molecules.
CN102211997A Alkannin naphthazarine mother nucleus acetoxylation derivative as well as preparation method and application thereof The invention discloses an alkannin naphthazarine mother nucleus acetoxylation derivative as well as a preparation method and application thereof, belonging to the technical field of medical chemistry. The structural formula of the alkannin naphthazarine mother nucleus acetoxylation derivative is shown in the specifications, wherein R is alkane, olefin, cyclane, cycloolefine or arene which contains 1-7 carbon atoms, or is alkane, cyclane, cycloalkane or arene which contains atoms; R1=R2=COCH3; and R3=R4=H or R1=R2=R3=R4=COCH3. Compared with alkannin, the invention has the advantages that: an in-vitro tumor cell suppression test indicates that the cytotoxicity is lowered, an animal in-vivo antitumor test indicates that the derivative has a certain tumor growth suppressing action, and the derivative can be used as a pre-medicament applied to the treatment of malignant tumors or the treatment of malignant tumors. Meanwhile, the preparation method related to the invention has the advantages of readily-available raw materials, short synthetic route and mild condition.
WO2005110444A1 Therapeutic or preventive agent for eye disease A therapeutic or preventive agent for eye diseases which contains spherical activated carbon as an active ingredient. The therapeutic or preventive agent is effective, without causing any side effect, for eye diseases such as cataract, retinopathy, glaucoma, macular degeneration, and retinal hemorrhage.
US20110177107 Predicting and reducing alloimmunogenicity of protein therapeutics Methods of predicting the immunogenicity of a therapeutic protein in a subject are provided and the use of this method in selecting a protein for replacement therapy having the fewest immunogenic epitopes. The method is demonstrated by reference to ADAMTS13. Isolated allelic variants of ADAMTS13 that contribute to the variability in risk for both arterial and venous thrombotic disease development are provided. The allelic variants are identified as single nucleotide polymorphisms (ns-SNPs) in the ADAMTS13 gene, which result in haplotypes identified as H1 to H14. A method for improving outcomes of transfusions/transplant products is also provided by selection of haplotype matched therapeutics.
US20100173893 Preparation of eslicarbazepine and related compounds by asymmetric hydrogenation A process for preparing a compound of the formula IA or IB: wherein R is alkyl, aminoalkyl, halogenalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkoxy, phenyl or substituted phenyl or pyridyl group; the term alkyl means carbon chain, straight or branched, containing from 1 to 18 carbon atoms; the term halogen represents fluorine, chlorine, bromine or iodine; the term cycloalkyl represents a saturated alicyclic group with 3 to 6 carbon atoms; the term aryl represents unsubstituted phenyl group or phenyl substituted by alkoxy, halogen or nitro group, the process comprising asymmetric hydrogenation of a compound of the formula II: wherein R has the same meanings as above, using a chiral catalyst and a source of hydrogen.
CN1771957A Bilobalide-containing medicine composition and its prepn and use The present invention belongs to the field of medicine technology, and is especially one kind of bilobalide-containing medicine composition and its preparation and use. The medicine composition contains bilobalide and ligustrazine phosphate in the amount of 1-100 times weight of bilobalide. The medicine composition has the synergistic effect of both bilobalide and ligustrazine phosphate, possesses functions of promoting blood circulation to disperse blood clots, resisting platelet aggregation, dilating blood vessel and improving microcirculation, and is applied in preparing medicine for treating ischemic cardiac and cerebral vascular diseases.
CN102266051B Antifatigue composition and preparation method thereof The invention provides an antifatigue composition and a preparation method thereof. The antifatigue composition comprises the following active ingredients in part by weight: 50 to 300 parts of rhodiola rosea extract, 50 to 300 parts of siberian ginseng extract and 500 to 5,000 parts of L-carnitine or pharmaceutically acceptable salts thereof. A test proves that when L-carnitine is cooperatively used with rhodiola rosea and siberian ginseng, the fatigue of a human body can be released and the synergism is achieved.
WO2008026310A1 Protective agent for oral mucosa containing trehalose The object of the invention is to provide a protective agent for oral mucosa for protecting the mucosa in the oral cavity from dry irritation. The object can be basically achieved by a protective agent for oral mucosa containing an effective amount of trehalose as an active ingredient. As demonstrated by Examples, according to the protective agent for oral mucosa of the invention, a dry condition in the oral cavity can be effectively prevented, therefore, in particular during surgery, the risk of receiving damage from dry irritation caused by drying the area undergoing surgery and its peripheral mucosa.
CN102649711A Extracting method for drumstick phenanthrene The invention relates to an extracting method for drumstick phenanthrene, which comprises the following steps of: crushing dendrobium plant drugs; performing ultrasonic or backflow extraction by taking 70-95% alcohol solution; concentrating the extracting solution, thereby obtaining a crude extract; dissolving the crude extract with 8-20 times of 20% alcohol; taking macroreticular resin from supernate; decolorizing by adding active carbon into eluent injection; filtering the active carbon; concentrating, thereby obtaining precipitate; washing the precipitate with petroleum ether, thereby obtaining crude product; separating and purifying the crude product by adopting a HSCCC (High Speed Counter Current Chromatography) method; and reducing pressure and drying the effluent, thereby obtaining the product. The method is simple in process for producing the drumstick phenanthrene; the purity is high; and the preparation volume is large.
CN103239421A Fluvastatin sodium composition capsule and preparation method thereof The invention relates to the field of medicaments, and discloses a fluvastatin sodium composition capsule; the medicament effective components prepared into one thousand capsules include 15 to 40grams of fluvastatin sodium, 20 to 50grams of microcrystalline cellulose, 120-250grams of lactose, 4 to 10grams of hydroxypropylcellulose, 50 to 100grams of 3% starch slurry and 0.5 to 2.5grams of magnesium stearate. The invention also discloses a preparation method of the fluvastatin sodium composition capsule. The fluvastatin sodium composition capsule provided by the invention has the characteristics of low cost, high absorption rate after being taken, excellent therapeutic dose tolerance of patients, light adverse reaction and the like, and is a safe and effective lipid lowering medicament; in the preparation method, the whole process is simple and the process control parameter is easy to control, and therefore the preparation method is suitable for large-scale industrialized popularization.
CN103043661A Method for preparing active carbon for relieving or neutralizing effect of alcohol The invention provides a method for preparing active carbon for relieving or neutralizing the effect of alcohol. The method comprises: using wood, shells, mao bamboo or coal as raw material, to customize active carbon with certain aperture distribution, of which the specific surface area is 1100-2000m2/g, refining the customized active carbon, and adding 8-20% of aqueous alkali and the active carbon into a reaction vessel; introducing steam to heat the aqueous alkali until the temperature rises to 90+-5 DEG C, insulating, and dehydrating when the temperature falls up to less than 55 DEG C; washing with tap water and then dehydrating for several times; adding the dehydrated material into 6-15% of acid solution for pickling, introducing steam to heat the acid solution until the temperature rises to 65+-6 DEG C, insulating, adding cold water, and dehydrating when the temperature falls up to less than 55 DEG C; washing with tap water and then dehydrating for several times; washing with pure water and then dehydrating, to regulate the pH value in a range of 6.5-9.5. The active carbon prepared by the method has an obvious effect for relieving or neutralizing the effect of alcohol, accords with the standard of GB/T 13803.4-1999 of activated carbon for refinement of injection and the standard of medicinal charcoal in the Chinese Pharmacopoeia: 2010 edition, and accords with an edible hygienic standard.
US20110218210 Compounds for treating abnormal cellular proliferation Provided herein are compounds, compositions and methods for treating disorders mediated by abnormal cellular proliferation and processes for identifying such compounds.
US7462617 Substituted acylpiperazine derivatives The invention relates to compounds of formula wherein the substituents are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention further relates to methods for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other d 1iseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
CN101361784A Combination containing brown alga polysaccharide sulfuric ester and pueraria root and use thereof The invention discloses a composite comprising fucoidan and radix puerariae which is an active ingredient with synergistic action. The composite can be used for drugs and health care products for preventing chemical liver injuries. Experiments show that drugs or the health care products applying the composite have accessorial effect on treating chemical liver injuries and enhancing disease-resisting capability when taken for a long term. The invention also discloses a preparation technique of the composite.
US20110086855 Novel compounds as cannabinoid receptor ligands and uses thereof The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
US20060052437 Combination of an hmg-coa reductase inhibitor and a nitrate ester The present invention relates to the therapeutical combination of an HMG-CoA reductase inhibitor (statin) and a nitrate ester and is useful mainly for the preparation of medicaments for the prevention and treatment of coronary diseases as myocardial infarction and cerebrovascular diseases as stroke. Particularly, as a nitrate ester, a nitrate prodrug of aspirin, salicylic acid or vitamin E is used. Said compositions, compared to single components, have the advantages to be without toxic effects, mainly due to statins, and to be more effective.
US20060014701 Novel amide derivatives as growth hormone secretagogues Disclosed are the novel compounds as growth hormone secretagogues represented by the structural Formula I: wherein R1 is, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, or substituted or unsubstituted amino, X is —CO— or —SO2—, Y is: wherein n is an integer from 0-4, R4 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, R5 and R6 are independently selected from hydrogen, substituted or unsubstituted alkyl, or R5 and R6 or R4 and R5 are taken together to form substituted or unsubstituted alkylene, R2 is hydrogen, or substituted or unsubstituted alkyl, R3 is substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, D is substituted or unsubstituted amino, substituted or unsubstituted alkoxy, or substituted or unsubstituted alkylthio, * represents an asymmetric center, and pharmaceutically acceptable salts and individual isomers thereof, which have growth hormone releasing activity in humans or animals.
US20120046269 Novel Amino Azaheterocyclic Carboxamides The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
WO2007007982A3 Glucose uptake modulator and method for treating diabetes or diabetic complications The present invention relates to a glucose uptake modulator selected from the group consisting of a lysophosphatidyl derivative and urocortin, a pharmaceutical composition comprising the same, and a method of treating diabetes or diabetic complications in a mammal in need thereof.
US20080124366 Methods and Compositions for Treating Tumors The present invention is based on the finding that toll-like receptor (TLR) agonists affect immune responses in a subject. The compositions and methods of the present invention include administering to the subject a therapeutically effective amount of a tumor lysate or tumor lysis agent in conjunction with a therapeutically effective amount of a TLR agonist.
CN100998412B Health-care food for preventing and treating senile constipation A health-care food for preventing and treating senile constipation is prepared from the sodium alginate extracted from edible seaweed and the glucomannan extracted from river giantarum.
DE102007048447A1 New substituted dihydropyrazole-3-thione compounds are hypoxia inducible factor-prolyl-4-hydroxylase inhibitor, useful for preparing medicament to treat and/or prevent e.g. cardiovascular diseases, wound healing and anemia Substituted 1,2-dihydro-pyrazole-3-thione compounds (I), and their salts, solvates or solvates of the salts, where (I) excludes 3-methyl-4-(3-methyl-1,2,4-oxadiazol-5-yl)-1-pyridin-2-yl-1H-pyrazol- 5-thiol, are new. Substituted 1,2-dihydro-pyrazole-3-thione compounds of formula (I) and their salts, solvates or solvates of the salts, where (I) excludes 3-methyl-4-(3-methyl-1,2,4-oxadiazol-5-yl)-1-pyridin-2-yl-1H-pyrazol- 5-thiol, are new. R 1>a heteroaryl-group of formula (a), (b), (c), (d), (e) or (f); A : CR 4>or N, where at most two A are N; D 1>O, S or NR 5>; E : CR 6>or N, where at most two E are N; R 2>heteroaryl of formula (i)-(xiii); G : CR 7>or N, where at most two G are N; J : O, S or NR 8>; L : CR 9>or N, where at most two L are N; R 4>, R 7>, R 9>H, halo, CN, NO 2, (1-6C)-alkyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5-6-membered heteroaryl or L 1>; R 5>, R 8>H, (1-6C)-alkyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5-6-membered heteroaryl (where in R 4>, R 5>, R 7>-R 9>: (1-6C)-alkyl is 1-3 times substituted by halo, CN, oxo, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5-6-membered heteroaryl, or L 1>, where cycloalkyl-, heterocycloalkyl-, phenyl- or heteroaryl are 1-3 times substituted by L 2>, and (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5-6-membered heteroaryl are 1-3 times substituted by (1-6C)-alkyl, halo, CN, oxo or L 1>where the alkyl is 1-3 times substituted by L 3>); R 10>, R 11>H, (1-6C)-alkyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5-6-membered heteroaryl, where (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5-6-membered heteroaryl are 1-3 times substituted by L 2>, and (1-6C)-alkyl is 1-3 times substituted by L 3>; R 12>, R 14>, R 15>, R 18>, R 20>, R 22>, R 25>-R 27>, R 29>-R 31>R 10>; and R 13>, R 16>, R 17>, R 19>, R 21>, R 23>, R 24>, R 28>, R 32>H or (1-6C)-alkyl 1-3 times substituted by halo, CN, OH, CF 3, (1-4C)-alkoxy, NH 2, (1-4C)-alkylamino, di-(1-4C)-alkylamino, COOH and/or (1-4C)-alkoxycarbonyl; or R 12>R 13>, R 15>R 16>, R 17>R 18>, R 19>R 20>, R 21>R 22>, R 22>R 23>, R 24>R 25>, R 27>R 28>, R 31>R 32>5-6-membered heterocycloalkyl ring (1-3 times substituted by L 2>); L 1>C(O)R 10>, C(O)OR 11>, C(O)NR 12>R 13>, OC(O)R 14>, OC(O)NR 15>R 16>, NR 17>C(O)R 18>, NR 19>C(O)OR 20>, NR 21>C(O)NR 22>R 23>, NR 24>SO 2R 25>, SO 2R 26>, SO 2NR 27>R 28>,-OR 29>, SR 30>or NR 31>R 32>; L 2>halo, CN, (1-4C)-alkyl, CF 3, OH, (1-4C)-alkoxy, CF 3O, oxo, NH 2, (1-4C)-alkylamino, di-(1-4C)alkylamino, COOH and/or (1-4C)-alkoxycarbonyl; L 3>halo, CN, OH, CF 3O, (1-4C)-alkoxy, NH 2, (1-4C)-alkylamino, di-(1-4C)-alkylamino, COOH, (1-4C)-alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-memebred heterocycloalkyl, phenyl and/or 5-6-membered heteroaryl; R 6>H, halo, CN, NO 2, (1-6C)-alkyl, CF 3, OH, (1-6C)-alkoxy, CF 3O, NH 2, (1-6C)-alkylamino, di-(1-6C)alkylamino, COOH or (1-6C)-alkoxycarbonyl; and R 3>H, 1-6C alkyl or (3-7C)-cycloalkyl. Independent claims are included for: (1) preparations of (I); and (2) a medicament comprising (I) in combination with an inert, non-toxic, auxiliary material and one or more active substances from angiotensin-converting enzyme or phosphodiesterase inhibitor, angiotensin II-receptor antagonist, beta-blocker, calcium-antagonist, mineralocorticoid receptor antagonist, diuretics, aspirin, iron supplements, vitamin B12 and folic acid supplements, statin, digitalis (digoxin)-derivative, tumor chemotherapeutics or antibiotics. [Image] [Image] [Image] [Image] [Image] - ACTIVITY : Cardiovascular-Gen.; Cardiant; Antianemic; Nephrotropic; Vulnerary; Antimicrobial; Anti-HIV; Antiinflammatory; Antiarthritic; Antirheumatic; Metabolic; Cytostatic; Ophthalmological; Cerebroprotective; Antiparkinsonian; Neuroprotective; Nootropic; Analgesic; Endocrine-Gen.; Antidiabetic; Vasotropic; Antianginal; Antiarteriosclerotic. - MECHANISM OF ACTION : Hypoxia inducible factor-prolyl-4-hydroxylase inhibitor. The ability of (I) to inhibit hypoxia inducible factor-prolyl-4-hydroxylase was te
CN103275106A Indole alkaloid adduct, and preparation method and application thereof in preparing anti-tumor drug The invention relates to the field of anti-tumor drugs, and specifically discloses an indole alkaloid adduct, and a preparation method and an application thereof in preparing an anti-tumor drug. The indole alkaloid adduct has a structure shown as a formula I, wherein R is formed in the way that an indole alkaloid is subjected to hydrazinolysis and the hydrazinolysis product is bonded with hydrazine group. The indole alkaloid adduct can significantly reduce toxicity to normal cells and in-vivo toxicity and inhibit in-vitro proliferation of various tumor cell lines and the growth of tumor in the nude mouse bearing the tumor.
WO2011046901A3 Broad spectrum antiviral and methods of use A method for the prevention or treatment of Influenza virus infection or Adenovirus infection by administering an effective amount of a compound of Formula (I)1 Formula (II), or similar compound to an individual in need is provided.
US20060183105 Human brain-derived tissue-specific potassium channel A novel human brain-derived potassium channel polypeptide is described which is developmentally regulated and tissue-specific to differentiated neurons. A full length cDNA which encodes the novel potassium channel polypeptide is disclosed as well as the interior structural region and the amino acid residue sequence of the human brain potassium channel biomolecule. Methods are provided to identify compounds that modulate the biological activity of the potassium channel biomolecule and hence regulate neurophysiology.
US20130040906 Inhibitors of Human EZH2, and Methods of Use Thereof The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
US20080305068 Cosmetic compositions having improved transfer resistance Cosmetic compositions and methods with improved transfer resistance and long wear properties are disclosed. The cosmetic compositions contain a synergistic combination of at least one silicone polyurethane polymer and at least one elastomer.
WO2014085633A1 Substituted biaryl sulfonamides and the use thereof Provided herein are substituted biaryl sulfonamide compounds of formula (I), pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate initiation of protein translation. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders.
CN1771921A Control releasing venlafaxine hydrochloride tablet and its prepn The present invention discloses one kind of control releasing venlafaxine hydrochloride tablet and its preparation process. The control releasing venlafaxine hydrochloride tablet consists of medicine core of venlafaxine hydrochloride and semi-permeable coating with pores. The medicine core consists of venlafaxine hydrochloride 75 weight portions, stuffing 30-250 weight portions, osmotic pressure promoter 1-50 weight portions, adhesive 1-20 weight portions and lubricant 0.1-20 weight portions. The preparation has reasonable composition, excellent control releasing effect, long effective time, less side effect on gastrointestinal tract, less differential personal effect, high safety and good compliance.
CN102657623A Andrographolide lyophilized powder injection and preparation method thereof The invention belongs to the technical field of pharmaceutical preparations, in particular relates to a stable andrographolide pharmaceutical composition which is lyophilized powder injection. The andrographolide pharmaceutical composition is characterized in that the lyophilized powder injection comprises a dextran and sodium chloride freeze-drying filler composition. The lyophilized powder injection prepared is more stable, and variation of relevant substances after long storage is small.
US7300645 Oral composition comprising isomalt and remineralizing enhancing agent Disclosed is an oral composition comprising palatinit. More particularly, disclosed is an oral composition comprising palatinit which exerts a synergistic effect when combined with a fluorine or zinc compound.
CA2602555A1 Composition and method for reducing inflammation The present invention relates to a composition and method for the simultaneous alleviation of the symptoms of inflammation brought about by innate immune responses wherein said composition acts by inhibiting leukotrienes, chemotactic cytokines and cyclooxygenases. The composition of the present invention comprises at least an extract of Butterbur, Bromelain and an extract of White Willow bark.
EP1462081B1 Production of ceramide emulsions Ceramide emulsions containing: (A) sphingosines having a specific structure; (B) an acidic compound selected from among inorganic acids and organic acids having a molecular weight of 200 or less; and (C) ceramides having a specific structure; but containing neither any acrylic polymers nor any phospholipids; skin preparations for external use comprising these ceramide emulsions; and a process for producing a ceramide emulsion.
US20080058420 A mixture of excipients not promoting the conversion of gabapentin into the corresponding lactamic impurity; including a sliding agent, e.g., calcium phosphate, a lubricant either hydrogenated castor oil or glyceryl tribehenate, and optionally a diluent saccharide; capsules; storage stability; nontoxic The present invention relates to pharmaceutical compositions comprising gabapentin and a mixture of excipients capable of not promoting the conversion of gabapentin into the corresponding lactamic impurity, processes for their preparation and capsules that contain said compositions.
US20100143289 Umbilical cord stem cell secreted product derived topical compositions and methods of use thereof Compositions including topical formulations comprising secreted products obtained from the culture medium of human umbilical cord stem cells and particular combinations of components therefrom are provided for treatment of various dermatological conditions, such as adverse consequences of aging, wrinkling, altered pigmentation, altered viscoelasticity, and altered thickness, among others. Methods for using the compositions and topical formulations for treating adverse or undesirable dermatological conditions are also provided, as well as preventing the appearance of undesirable dermatological conditions.
WO2011156479A3 Trkb agonists and methods of use Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.
US20060009465 Treatment of sleep disorders using sleep target modulators The invention is directed to compositions used for treating sleep disorders. In addition, the invention provides convenient methods of treatment of a sleep disorder. Furthermore, the invention provides methods of treating sleep disorders using compositions that remain active for a discrete period of time to reduce side effects. More specifically, the invention is directed to the compositions and use of ester derivatized trazodone compounds for the treatment of sleep disorders.
CN102325778A Nalmefene hydrochloride dihydrate The present invention relates to the Nalmefene hydrochloride dihydrate, methods of manufacturing Nalmefene hydrochloride dihydrate, a pharmaceutical composition comprising Nalmefene hydrochloride dihydrate and a method of treatment comprising administering Nalmefene hydrochloride dehydrate.
CA2552493A1 Methods for producing interfering rnas The present invention relates to gene silencing, and in particular to methods of synthesizing microRNAs (miRNAs) and short interfering RNAs (siRNAs) in vitro and in vivo, and to methods of using such to regulate gene expression.
US20100099771 Use of cooling agents to relieve mild ocular irritation and enhance comfort Ophthalmic compositions containing very low concentrations (e.g., 1 to 50 ppm) of cooling agents are described. The cooling agents are less volatile and less prone to causing ocular discomfort than agents previously utilized to obtain an ocular cooling effect, such as menthol. The cooling agents are preferably contained in a vehicle that forms a gel or partial gel upon application to the eye.
WO2012089738A1 A combination of an opioid agonist and an opioid antagonist in the treatment of parkinson's disease The present invention provides a pharmaceutical dosage form comprising an opioid agonist and an opioid antagonist for use in the treatment of Parkinson's disease. The present invention also refers to the use of an opioid agonist and an opioid antagonist in such a dosage form.
US20080206335 Inert non-pareil core, fluvoxamine layer over core, rate-controlling membrane coating; fluvoxamine released over a period of 12 hours or more; once-daily oral administration A multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) formulation for oral administration comprises particles of said SSRI or a pharmaceutically acceptable salt thereof coated with rate-controlling polymer which allows controlled release of said SSRI, over a period of not less than about 12 hours following oral administration. The formulation, which contains for example fluvoxamine or a pharmaceutically acceptable salt thereof, is suitable for once or twice daily administration. The formulation can comprise a blend of two or more populations of particles, pellets or mini-tablets having different in vitro and/or in vivo release characteristics.
CN102114175A Compound preparation for treating acute mastitis of milk cow The invention relates to a compound preparation for treating acute mastitis of a milk cow and the preparation method thereof. The composition mainly comprises lincomycin hydrochloride, houttuynia, honeysuckle flower, weeping forsythia fruit, dandelion, Chinese angelica root, luffa, ricepaper plant pith, cotton rose hibiscus leaves, chekiang fritillary bulb, cosolvent, preservative and proper amount of water for injection. The composition provided by the invention has the advantages of quick action and small irritation, is not easy to generate drug tolerance, and is used for treating both principal and secondary aspect of disease. The prepared compound preparation is injection which is convenient for application and easy for operation and can be easily accepted by farmers.
US20110217373 Extended release pharmaceutical compositions of guanfacine hydrochloride The present invention relates to an extended release pharmaceutical tablet composition comprising guanfacine comprising: a core containing guanfacine or a pharmaceutically acceptable salt thereof and one or more of pH-independent rate controlling polymer(s) and other pharmaceutically acceptable excipients; optionally a coating over the core as in (a) wherein, the coating comprises one or more of pH-independent rate controlling polymer(s).
US20110281906 Sustained release formulation for tacrolimus A sustained release pharmaceutical composition for tacrolimus, comprising a solid dispersion containing tacrolimus or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a dissolution rate of tacrolimus after 4 hours from the beginning of a dissolution test is less than 35%, is disclosed.
EP2473488A1 Substituted heterocyclic derivatives for the treatment of pain and epilepsy Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel activity, particularly unwanted Nav 1.7, Nav 1.8, or Cav 3.2 channel activity are disclosed. Specifically, a series of compounds containing piperidine or piperazine linked through an amide, isoxazole or similar linker to an aryl ring are described and are shown to be useful for the treatment of pain or epilepsy. A is selected from Formulae (i) or (ii).
WO2009136370A1 Parenteral supplement with traceelemξntsfor treatment of i. a. sirs, burns selenium-defenciencies The present invention addresses the problem of acute deficiencies of trace elements observed in critically ill patients and/or patients receiving parenteral nutrition - toxicity issues are intergrated. In order to solve the problem, the invention provides a kit for parenterally administrating trace elements to a patient, the kit comprising a basic unit of trace elements and at least one supplementary unit, the supplementary unit comprising supplementary trace elements so as to address the specific needs in trace elements of a specific patient. According to an embodiment, the invention provides a supplementary unit for patients diagnosed with SIRS, suffering from burns, patients on continuous renal replacement therapy and patients residing in selenium-poor countries.
US8664382 Antibacterial compositions comprising metal phthalocyanine analogues The present invention relates to pharmaceutical compositions comprising metal phthalocyanine analogues of formula (I) and metal chelating compounds having a good bioavailability and enhanced photoinactivation properties against Gram negative bacteria; and to their use for in vivolex vivo applications, such as blood and blood derivatives sterilization.
US20120058961 Pharmaceutical Composition for Treating Cancers The preset invention relates to a new approach for treating cancer by using a synergistic combination of a histone deacetylase inhibitor and a furost-5-ene-3,22,26-triol glycoside. A pharmaceutical composition for treating a cancer comprising the synergistic combination and the treatment of a cancer with the synergistic combination are provided.
CN103724359A Amorphous cefotetan acid, method for preparing cefotetan disodium by amorphous cefotetan acid and pharmaceutical composition containing cefotetan disodium The invention discloses a novel crystal form of cefotetan acid, a method for preparing cefotetan disodium by the novel crystal form of the cefotetan acid and a pharmaceutical composition containing the cefotetan disodium. The X-ray diffraction pattern of the novel crystal form appears no X-ray diffraction peak; the endothermic peak in the differential thermal analysis pattern is positioned at 158.3 DEG C; the exothermic peak is positioned at 144.6 DEG C. The novel crystal form solves the technical problem of instability of the cefotetan disodium prepared by using the cefotetan acid in the prior art. The used preparation method has good operability and few residues of organic solvent, and is specifically suitable for large-scale industrial production.
WO2006038526A1 Acid addition salt of irinotecan An irinotecan acid addition salt which comprises an acid selected from the group consisting of sulfuric acid, nitric acid, phosphoric acid, methanesulfonic acid, citric acid, maleic acid, and succinic acid and irinotecan which has added the acid; a process for producing the addition salt; and a medicinal composition containing the addition salt. The addition salt does not necessitate heating during medicinal-preparation production and gives an aqueous solution preparation in which the salt is in the state of being stably dissolved in the water.
US20080015258 Dissolving moprolol and tartaric acid in a 2:1 molar ratio in ethanol, precipitating and filtering; gels ointments, eyedrops; glaucoma; improved tolerability over hydrochloride salt L-(−)-moprolol L-(+)-tartrate salt (2:1), method for preparing it and pharmaceutical composition comprising it.
US20100331288 Crystalline hydrate of betamimetika and use as medicament thereof The present invention relates to a crystalline, enantiomerically pure hydrate of R-6-hydroxy-8-{1-hydroxy-2-[2-(4-methoxy-phenyl)-1,1-dimethyl-ethylamino]-ethyl}-4H-benzo[1,4]oxazin-3-one-hydrochloride of formula (1) and its activity as a long-acting betamimetic, on its own or combined with one or more other active substances for treating respiratory complaints.
CN1524517B Oral medicament composition containing non-steroid antiphlogistic drugs and its preparation method The invention provides an acetate type antiphlogistic medicine, in particular the oral medication composition of ketorolac comprising a core, pharmaceutical film (including medicament, adhesive and cracking layer) protecting layer, and a casing foil. The oral medication composition has shown specific effectiveness for treating aching patients of medium to severe degree. The invention also providesthe process for preparing the medicinal composition and the method for using the same.
CN102940682A Drug for treating esophagus cancer and stomach cancer The invention discloses a drug for treating an esophagus cancer and a stomach cancer and belongs to the field of medicines. The drug comprises rabiagar, centipede, nux vomica, scorpion, red sage root and inner membrane of chicken gizzard and can be used for treating an esophagus cancer and a stomach cancer.
US20120035206 Preparation and application of novel antibacterial and anticancer compounds and their derivatives Novel antibiotic and anticancer compounds of formula I, II, III, IV, derivatives, ostereoisomer, racemic and noracemic mixture of ostereoisomer, or the pharmaceutically acceptable salts or solvates of these compounds are disclosed. The preparation, pharmaceutical composition and biological activity of these compounds are disclosed.
EP1879884A1 Azole-based phosphodiesterase inhibitors The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds of Formula (I), pharmaceutical compositions containing the compounds described herein and their use as PDE type IV selective inhibitors are provided.
CN103040749A Sarpogrelate hydrochloride lipidosome solid preparation The invention relates to a sarpogrelate hydrochloride lipidosome solid preparation and a preparation method thereof. The preparation method comprises the following steps: selecting sarpogrelate hydrochloride, dilauroyl phosphatidylcholine, phosphatidyl ethanolamine, phosphatidyl glycerol and cholesterol with specific weight ratio to prepare sarpogrelate hydrochloride lipidosome with excellent quality; and preparing the solid preparation by the common preparation method. Compared with the conventional preparation, the preparation provided by the invention improves the stability, the bioavailability and the product quality of the preparation and reduces the toxic or side effect.
EP1268444B1 2,4-di(hetero-)arylamino(-oxy)-5-substituted pyrmidines as antineoplastic agents Pyrimidine derivatives of the formula (I), wherein: Q1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one or both Q1 and Q2 are substituted on a ring carbon by one substituent of the formula (Ia) or (Ia'), wherein : Y, Z, n, m, Q3, G, R1, are as defined within; and pharmaceutically acceptable salts and in in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.
US7439248 5-[[4-[3-Methyl-4-oxo-3,4-dihydro-2-quinazolinyl]methoxy]phenyl-methyl]thiazolidine-2,4-dione or salt; compressed tablets; microcrystalline cellulose, magnesium stearate, lactose, or talc excipients; antidiabetic agents for non-insulin dependent diabetes; insulin sensitizers The present invention provides a new stable pharmaceutical composition containing 5-[[4-[3-Methyl-4-oxo-3,4-dihydro-2-quinazolinyl]methoxy]phenyl-methyl]thiadiazolidine-2,4-dione as active ingredient.
EP2164827A2 Novel derivatives of 3-phenyl acrylic acid activating ppar-type receptors, method for preparing same and use thereof in cosmetic or pharmaceutical compositions The invention relates to novel derivatives of 3-phenyl acrylic acid of the following general formula (I), to a method for preparing the same, and to the use thereof in pharmaceutical compositions used in human or veterinary medicine (in dermatology as well as in the field of cardio-vascular diseases, immune diseases and/or diseases related to lipid metabolism), or in cosmetic compositions.
WO2010051935A3 Substituted amido phenoxybenzamides The present invention relates to substituted amido phenoxybenzamide compounds of general formula (I) in which A, R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
EP1501547A1 Methods and conpositions for treating, preventing or delaying onset of a neoplasm Methods of treating, preventing or delaying onset of a neoplasm comprise administering to an individual an anti-neoplastic agent and a growth hormone receptor antagonist. Methods for reducing tumor weight or volume comprise administering to an individual an anti-neoplastic agent and a growth hormone receptor antagonist. Compositions comprise an anti-neoplastic agent and a growth hormone receptor antagonist.
WO2012088038A2 Piperazinone-substituted tetrahydro-carboline mch-1 antagonists, methods of making, and uses thereof The present invention relates to piperazinone-substituted tetrahydro- carboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
CN1977879A Method for preparing bitter gourd cream and bitter gourd cream product The present invention relates to a preparation method of bitter melon cream and bitter melon cream product. The preparation method of bitter melon cream includes the following steps: slicing bitter melon, soaking said sliced bitter melon and mirabilite, boiling them to obtain white crystal powder product. Said bitter melon cream, other medicine and proper auxiliary material are mixed, and can be made into various dosage forms of tablet, dripping pills, powder preparation, granules, syrup, capsule, oral liquor and medicinal toothpaste, etc.
US8691291 System and method for patient preparation A method for preparing the human bowel to undergo colonoscopy. A salt solution, preferable having a 0.9% w/v concentration of sodium chloride in water and warmed to 40 C. degrees, is utilized. A series of twisting and maneuvering exercises, such as those used in Yoga, is also performed. A predetermine quantity of the salt solution is consumed during predetermined intervals between the exercise steps, intending to clear and cleanse the colon so as to prepare it to undergo colonoscopy within about 3 to 24 hours after the completion of the preparation.
CA2214033C Oral pharmaceutical dosage forms comprising a proton pump inhibitor and a prokinetic agent An oral pharmaceutical dosage form comprising a proton pump inhibitor and one or more prokinetic agents in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of multilayered tablets, capsules or multiple unit tableted dosage forms. The multiple unit dosage fortes are most preferred. The new fixed formulation is especially useful in the treatment of disorders associated with gastro oesophageal reflux diseases.
US20130052161 Inhibitors of flaviviridae viruses Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections (e.g. hepatitis C infections), particularly drug resistant Flaviviridae virus infections.
CN101199494A Kinesia-prevention patch and preparing method thereof The invention relates to a medical plaster used for motion sickness prevention and cure and the related preparation method. The plaster comprises a medical adhesive layer, a protective layer and a back lining layer and is made of the effective ingredients of scopolamine, polymer polyisobutylene B100, laurocapram polymer polyisobutylene B10 (dry weight), liquid paraffin and cyclohexane. The plaster has a three-layer structure, including the medical adhesive layer, the protective layer and the back lining layer. Each plaster contains 0.1 mg to 5 mg of scopolamine. According to quality inspection, the invention is even in content and stable in quality, with external release approaching zero-degree rate process. The invention can be used to prevent and cure motion sickness and has obvious effects.
CN101569619B New use of glyoxal bis (thiosemicarbazone) compound The invention discloses new use of glyoxal bis (thiosemicarbazone) compound. The new use relates to an application of glyoxal bis (thiosemicarbazone) compound or salt or a solvate of the compound in antineoplastic drug preparation. The glyoxal bis (thiosemicarbazone) compound of the invention can effectively kill a large number of tumour cells and dosage-effect relation and time-effect relation are obvious. Thus, the invention provides a new way for practice and research of tumour treatment and/or relapse prevention and also can be taken as reagent used for experimental researches relevant tocell cycle, cell proliferation, and apoptosis as well as a certain of signal passage regulation and control. The invention has wide application in tumour treatment and relapse prevention.
US20090226422 Chemical Inhibitors of Inhibitors of Differentiation The present invention provides identification of inhibitors of inhibitors of differentiation (Id) for use in the treatment and prevention of diseases in mammals. The inhibitors of Id are effective alone in the treatment of a variety of cellular proliferative disorders including, but not limited to, diseases such as cancer, arthritis, age-related macular degeneration, psoriasis, neoplasms, angiomas, endometriosis, obesity, age-related macular degeneration, retinopathies, restenosis, scaring, fibrogenesis, fibrosis, cardiac remodeling, pulmonary fibrosis, scleroderma, failure associated with myocardial infarction, keloids, fibroid tumors and stenting. Additionally, these compounds are effective in blocking angiogenesis in tumor development, inducing apoptosis in malignant cells, inhibiting proliferation of cancer cells, increasing the effectiveness of chemotherapeutic agents, regulating transcriptional activity, reducing inflammation, increasing cellular differentiation, modulating ETS domain transcription factors, modulating PAX transcription factors, modulating TCF-ETS domain transcription factors, down regulating RAF-1/MAPK, upregulating JNK signaling pathways, and modulating cellular transformation.
US20110104052 Methods of synthesis and use of chemospheres The present invention provides, in general, compositions comprising a hydrogel and an agent, for example a therapeutic agent or an imaging agent, for locoregional delivery. In certain preferred embodiments of the invention, the hydrogel compositions are detectable by Magnetic Responance and CT Scan and are used for locoregional delivery of therapeutic agents, for example chemotherapeutic agents. The invention also features polymer matrix compositions comprising nanoparticles that can be loaded after polymerization with bioactive agents, for example a diagnostic agent or therapeutic agent.
US20050238635 Use of hyrogen peroxide producting enzyme for treatment of otitis media The present invention relates to the use of hydrogen peroxide producing enzyme for manufacturing of a medicament for treatment and/or prevention of otitis media (inflammation in the middle ear), preferably in children. This enzyme is preferably NADH oxidase. The medicament is intended to be administered with lactoperoxidase into the nasal cavity.
WO2014153529A1 Substituted benzimidazoles as nociceptin receptor modulators The invention provides modulators of the nociceptin receptor (NOP), including both agonists and antagonists. A compound of the invention can be a selective modulator of NOP with respect to the μ- and κ- opioid receptors (MOP and KOP), thus providing a therapeutic method for the treatment of conditions wherein selective NOP modulation is medically indicated and MOP or KOP modulation may be less desirable. A compound of the invention can be a NOP full agonist, partial agonist, inverse agonist, positive or negative allosteric modulator, or a functionally biased agonist. A compound of the invention can be used for the treatment of an anxiety state, post-traumatic stress disorder, addictive disorders (including overuse of alcohol, tobacco, and drugs of abuse such as cocaine, amphetamines, and opitates), misregulated food intake and/or energy expenditure, cough, sleep disorders, migraine, pain, depression, or neurodegenerative disorders such as Parkinsons disease or Alzheimers disease.
EP1261330B1 Method for increasing intestinal absorption of fat soluble vitamins in post-menopausal women and in lower animals Applicants have discovered that L-carnitine increases the intestinal (lymphatic) absorption of fat soluble vitamins, such as vitamins A, D, and E, in post-menopausal women. As a result, L-carnitine enhances the antioxidant defense mechanism and lowers the risk of certain degenerative diseases, such as coronary heart disease, age-related macular degeneration, osteoporosis, cancer, and Alzheimer's, in post-menopausal women. The present invention provides a method for increasing the intestinal absorption, cellular concentration, biliary secretion, hepatic storage, and/or liver concentration of a fat soluble vitamin in a post-menopausal woman. The method comprises orally administering to a post-menopausal woman in need thereof, a fat soluble vitamin and a fat soluble vitamin absorption increasing effective amount of L-carnitine. The invention also provides a method for increasing the intestinal absorption of a fat soluble vitamin in an animal. The method comprises orally administering to the animal in need thereof, a fat soluble vitamin and a fat soluble vitamin absorption increasing effective amount of L-carnitine.
EP2576545A1 Nitrate and diazeniumdiolate derivatives of pioglitazone Nitrate ester and diazeniumdiolate derivatives of pioglitazone are described. They have valuable properties in the treatment of vascular and metabolic diseases, for example type 2 diabetes.
WO2013117285A1 Furo [3, 2 - b] - and thieno [3, 2 - b] pyridine derivatives as tbk1 and ikk inhibitors Compounds of the formula (I) in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TBK1 and ΙΚΚε and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
CN101416974A Preparation method of doxycycline long-acting injection The invention discloses a doxycycline long-acting injection which has the formula as follows: 5g to 20g of doxycycline, 10g to 60g of propylene glycol, 2g to 4g of MgCl2, 0.2g to 0.5g of Na2S2O5, and water used for injection. The preparation method comprises the following steps: 1. the doxycycline is added into the propylene glycol to obtain a solution (1); 2. the doxycycline hydrochloride, the MgCl2 and the Na2S2O5 are taken and dissolved in the water used for injection to obtain a solution (2); 3. the solution (2) is slowly added into the solution (1) and stirred while being added, and ethylene diamine is used for regulating the pH value to be 7.5 to 8.5; and 4. the water used for injection is added till the total volume reaches 100ml, and filtering, encapsulation and flowing steam sterilization at the temperature of 100 DEG C for 30min are carried out to obtain the finished product. The doxycycline long-acting injection has the advantages of less dosage, long half-life period, less adverse reaction, and the like.
CN101095695A Liposome artificial tear eye drops The invention relates to an artificial eye tear drop of liposome for preventing and treating dry eye disease and eye fatigue, which comprises soybean lecithin, cholesterin, anti-oxidizing agent and artificial tear hydrated liquid, whose constituents include sodium hydrogen carbonate, sodium chloride, glucose, potassium chloride, water, or one or more auxiliary compositions of mint, PVP and HPMC.
CN103520272A Drug for treating coronary disease and stenocardia The invention relates to a drug prepared from Chinese Tibet herbal medicine materials in Tibet plateau for treating coronary disease and stenocardia. The drug is prepared from the following crude drugs in parts by weight: 95-105 parts of seabuckthorn flavones, 5-10 parts of root of red-rooted salvia, 1-5 parts of ligusticum wallichii, 15-25 parts of talcum powder, and 1-3 parts of fructus podophylli. The drug can be used for restoring veins and removing thrombosis, circulating vital energy and blood, and supplying blood and vital energy, and is applicable to treatment of dragon-type stenocardia, blood-type stenocardia, an ischemic heart disease, coronary disease, atherosclerosis, myocardial infarction and arrhythmia, and reduction of cholesterol and hyperlipidemia.
US7879335 Glycoconjugates, glycoamino acids, intermediates thereto, and uses thereof The present invention provides novel n-alkenyl glycosides and glycoconjugates, n-alkyl glycoamino acids, and methods for the synthesis thereof. In another aspect, the present invention provides novel clustered glycopeptides and methods for the synthesis thereof. In still another aspect, the present invention provides methods for the treatment of cancer, preferably for the prevention of recurrence of cancer, and methods for inducing antibodies in a subject, comprising administering to a subject in need, an effective amount of any of the inventive glycoconjugates as disclosed herein.
CN1823995A New medicine for treating malignant tumour A medicine for treating cancer is prepared from aspirin powder, chloroquinoline, testosterone, and 22 Chinese-medicinal materials including ginseng, houttuynia herb, honeysuckle flower, astragalus root, etc.
US20090270454 Sulfonamide containing compounds for treatment of inflammatory disorders Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof: wherein: X and Y are independently selected from —CH2— or —CH2—CH2—; Z is selected from S(O)m or Se(O)m and m is 0, 1 or 2; R1 is optionally substituted heteroaryl or heterocyclic; R2 is selected from the group consisting of hydrogen, C1-C6 straight alkyl, and C1-C6 branched alkyl, wherein all may be optionally substituted; and R3 and R4 are alkyl.
WO2011033009A1 N- [2-hydroxycarbamoyl-2- (piperazinyl) ethyl] benzamide compounds, their preparation and their use as tace inhibitors The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I), and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.
US6930104 beta -amyloid precursor protein secretory stimulators; treating neurodegenerative disorders; n-carbamoyl- quinoxaline or quinoline derivatives The object of the present invention is to provide soluble β-amyloid precursor protein secretory stimulators, which are effective in treating neurodegenerative diseases as well as cerebrovascular disorder-induced neuronopathy. More specifically, the present invention provides a novel compound of the following Formula (I) or a salt or prodrug thereof: [wherein R1 and R2 each represent a hydrogen atom or a lower alkyl group, etc., Ar1 and the ring B each represent an optionally substituted aromatic group, the ring A represents an optionally substituted benzene ring, the ring C represents an optionally substituted 4- to 8-membered ring which may further be condensed with an optionally substituted ring, X represents CH or N, and Y represents CH or N].
US20120028935 Therapeutic Gestagens for the Treatment of Premenstrual Dysphoric Disorder A method of treating premenstrual dysphoric disorders comprising administering to a patient in need of such treatment daily from day 1 to day 24 3 mg of drospirenone and 0.02 mg of ethinylestradiol.
EP2266579A1 Pharmaceutical composition comprising elvucitavine A pharmaceutical composition comprising elvucitabine, lactose monohydrate, and anhydrous lactose, in which the lactose monohydrate and anhydrous lactose taken together comprise about 60 percent to about 90 percent of the pharmaceutical composition by weight.
WO2007086526A1 Gene polymorphism and use thereof It is intended to provide a method of estimating the prognosis of cancer, in particular, ovary cancer, uterine corpus cancer and lung cancer, by examining a polymorphism (-202G/C and +20A/C) occurring in the 5’-regulatory region of LTBP-1L gene; and a method of treating cancer, in particular, ovary cancer, uterine corpus cancer and lung cancer, by inhibiting the expression or activity of LTBP-1L. It is also intended to provide a method of predicting the sensitivity to uterine corpus cancer, gastric cancer and lung cancer by examining the polymorphism as described above.
EP2318366A2 Psma-binding agents and uses thereof Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.
WO2010128152A1 Fused heterocyclic c-glycosides for the treatment of diabetes The present invention provides compounds of Formula (IA) wherein A is selected from Formula (II) which have an inhibitory effect on the sodium dependent glucose transporter SGLT and their use in the treatment of diabetes.
US20090130197 Extended release pellet formulation containing pramipexole or a pharmaceutically acceptable salt An extended release pellet comprising an active ingredient selected from pramipexole and the pharmaceutically acceptable salts thereof, and at least one release-modifying excipient.
EP1549309A2 Somatostatin analogue compounds Compounds having somatostatin activity of the following Formula I, wherein, R1 is aryl, substituted-aryl, and aryl(lower-alkyl)-; R2 is lower alkyl, amino substituted lower alkyl, -carboxy-(lower-alkyl), -carbamic acid-(lower alkyl) and -carboxy-(lower-alkyl)-aryl; and R3 and R4 are independently, lower-alkyl, aryl, substituted-aryl, (substituted-aryl)-(loweralkyl)-, heteroaryl, (heteroaryl)-(lower-alkyl)-, substituted-heteroaryl, (substituted heteroaryl)-(lower-alkyl)-, heterocyclic, heterocyclic-(lower-alkyl)-, substituted-heterocyclic, (substituted-heterocylic) -(lower alkyl)-, -carboxy-(lower-alkyl), and -carboxy-(lower-alkyl)-aryl; or a pharmaceutically acceptable, ester, ether, or salt thereof; methods for their use; and preparation.
WO2007058336A1 SCREENING METHOD AND IDENTIFICATION METHOD FOR SUBSTANCE CAPABLE OF INHIBITING DEGRANULATION REACTION OR PROSTAGLANDIN D2 PRODUCTION IN MAST CELL THROUGH Rec168, AND THERAPEUTIC AGENT FOR INFLAMMATORY DISEASE COMPRISING THE SUBSTANCE The object is to provide: a method for screening a substance capable of regulating degranulation or inhibiting prostaglandin D2 production; and a method for identification of a substance capable of inhibiting the degranulation or prostaglandin D2 production in a mast cell, these methods being useful for developing a therapeutic agent for an allergic disease or an autoimmune disease based on a new mechanism through a G-protein conjugated receptor Rec168. Disclosed is a method for screening of a substance capable of inhibiting the signal transduction capability or a substance capable of regulating the degranulation or inhibiting the prostaglandin D2 production in a mast cell through Rec168. The method comprises the steps of: determining the signal transduction capability of a ligand having a Rec168-agonistic activity toward Rec168 in the presence or absence of a substance to be tested; and comparing a measurement value obtained in the presence of the substance with a measurement value obtained in the absence of the substance. Also disclosed is a method for identification of a substance capable of inhibiting the degranulation or prostaglandin D2 production in a mast cell.
WO2007006922A8 Novel 1h-indole-pyridinecarboxamide derivatives and 1h-indole-piperidinecarboxamide and their use as hydroxylase tyrosine inducers The invention relates to compounds of formula (I), to their enantiomers, diastereoisomers, N-oxides, as well as to their pharmaceutically acceptable acid or base addition salts. The inventive compounds are hydroxylase tyrosine inducers.
CN1874757B Mucoactive agents for treating a pulmonary disease The present invention relates to mucoactive agents, such as heparin which are useful in the treatment of diseases where excess mucus is present in the respiratory tract, such as cystic fibrosis and chronic obstructive pulmonary disease. In particular, the invention relates to pharmaceutical compositions for administration by pulmonary inhalation. It also relates to methods for producing particlessuitable for pulmonary inhalation, such as spray drying or jet milling.
WO2013150153A1 Ketone bodies and ketone body esters for maintaining or improving muscle power output Ketone bodies and ketone body esters maintain or improve muscle power output upon oral administration. Certain esters of hydroxybutyrate monomers are organoleptically acceptable and have high levels of uptake from the gut to the blood thereby allowing a rapid increase of blood concentration of hydroxybutyrate and beneficial physiological response including improved power output during exercise. Compositions containing the ketone bodies or ketone body esters are also described.
US20050106679 Leptin proteins This invention relates to novel protein INSP035, herein identified as a member of the four helical bundle cytokine family and to the use of this protein and the nucleic acid sequence from the encoding gene in the diagnosis, prevention and treatment of disease.
EP2275411A2 Reformatsky Reagent in Stable Form and Process for Producing the Same The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I): and a Reformatsky reagent in a stable form suitable for the process. In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5·THF)2.
CN102038838A Externally-used drug for treating bone fracture The invention provides an externally-used drug for treating bone fracture, which is prepared from rehmannia, radix angelicae, dragon's blood, centipede, balsam, muskiness, native copper and rhizoma drynariae at a certain proportion. The drug has the efficacies of destroying bacteria and diminishing inflammation, knitting bone and relaxing tendons, dredging collateral and promoting tissue regeneration and relieving pain, can be used for treating the bone fracture and injuries from falls, and has the advantages of fast relieving pain, short course of treatment, fast recovery and low drug price.
US20100092400 Salicylic Acid Composition Provided, among other things, is a delivery module for water-based salicylic acid composition comprising: an aerosol delivery system; within the aerosol delivery system, the salicylic acid composition comprising 0.5% or more salicylic acid by weight, lipophilic component(s), and a frothing agent, the salicylic acid composition having a viscosity low enough to support aerosol delivery, and the salicylic acid composition effective to form a foam upon propellant-driven aerosol delivery; and within the aerosol delivery system, a propellant, wherein the salicylic acid composition is non-irritating and has a non-watery feel.
WO2006107253A1 Novel diazaspiroalkanes and their use for treatment of ccr8 mediated diseases The invention provides compounds of general formula wherein R and R1 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
CN102643247A Disulfide compound as well as preparation method and application thereof The invention belongs to the fields of organic chemistry and pharmaceutical chemistry and particularly relates to novel disulfide compounds shown as a formula I as well as a synthetic method and application of the novel disulfide compounds. The disulfide compounds have strong inhibiting function for various tumor cells and can be used as pilot compounds for researching novel tumor-resisting medicaments or can be used as medicaments for treating various clinically-general multiple cancers. The formula I is shown as the description.
US7732617 Tocopherol derivatives and uses thereof Tocopherol derivatives having the general formula: wherein n is an integer of 6 to 13, R1 is hydrogen, a silyl ether or acetate, R2 is an optionally substituted nitrogen-containing heterocycle or a polycyclic nitrogen-containing heterocycle; and pharmaceutically acceptable salts thereof are provided. A method for synthesizing the compounds is also provided. The tocopherol derivatives are capable of inhibiting the primary enzyme responsible for the metabolism of the tocopherols and tocotrienols compounds of vitamin E, namely tocopherol-ω-hydroxylase, and thus increase the amount and prolong the availability of these compounds in plasma and tissue.
CN102895204A Sevelamer carbonate crude drug for preparing tablets, preparation method and application thereof The invention belongs to the field of pharmacy, and relates to a sevelamer carbonate crude drug for preparing tablets, a preparation method and application of the sevelamer carbonate crude drug. The particle size of the sevelamer carbonate crude drug meets the conditions: D 0.95 is less than or equal to 180mu m, D 0.50 is less than or equal to 50mu m, and D 0.05 is more than or equal to 9mu m at the same time. The polyallylamine carbonate has the soluble oligomer (0.2%) within the particle size range. The tablets prepared from the sevelamer carbonate crude drug have the advantages of being smooth in surfaces, good in hardness and low in friability.
CN102153471A Idebenone succinate monoester and preparation method thereof The invention relates to an idebenone succinate monoester and a preparation method thereof. Idebenone is a novel specific medicine for resisting senile dementia and an improver for improving the brain function and metabolism and psychotic symptoms and has multiple pharmacological effects. The idebenone has disadvantages of not being soluble in water and being only administrated orally. The idebenone succinate monoester disclosed by the invention has a structural formula shown in the specification, is soluble in both organic solvents and water and has better stability in water. When the idebenone succinate monoester is converted into corresponding water-soluble salts, the solubility of the idebenone succinate monoester in water can be improved further. The preparation method comprises the following steps of: dissolving idebenone and succinic anhydride (butanedioic anhydride) in an organic solvent, reacting at 0-100 DEG C under the catalysis of an alkaline substance for 1-1000h, removing the alkaline substance used as a catalyst with acid or acid salt to finally obtain the high-purity idebenone succinate monoester which is suitable for large-scale production. The compound and the corresponding water-soluble salts thereof can be prepared into both oral preparations and injections, and therefore, the application range of idebenone is greatly expanded.
WO2008135578A1 Pyrazolo [3, 4-d] pyrimidine derivatives for the treatment of inflammation and/or allergic conditions The present invention provides compounds of formula (I): a process for their preparation, pharmaceutical compositions comprising the compounds and the use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation and/or allergic conditions.
US20100197791 Pharmaceuticals for transdermal use on animals The invention relates to pharmaceutical preparations for use on animals, which are applied to the fur or the skin of the animal and whose active ingredient subsequently undergoes transdermal absorption.
US20070232643 Quinoline derivative, e.g. 2[4-(7-chloroquinolin-2-yloxy)phenoxy]propionic acid sodium salt; anticarcinogenic, antitumor agent; colon, breast, melanoma, pancreatic cancer or adenocarcinoma; melanoma, or leukemia; based on herbicides The invention provides compounds of formula I: wherein Y is F, Cl, Br, methyl or methoxy; and pharmaceutically acceptable salt thereof. The compounds are effective antitumor agent. The invention also provides pharmaceutical compositions comprising a compound of formula I or a salt thereof, intermediates useful for preparing a compound of formula I, and therapeutic methods comprising administering a compound of formula I or a salt thereof to a mammal in need thereof.
WO2007128482A1 Use of a b-cell-depleting antibody for treatment of polyoma virus infections The present invention relates to uses of a B-cell-depleting antibody for the treatment of a polyoma virus infection.
US7605274 precipitating crystalline form from solvent solution using water as an antisolvent This invention relates to an improved process of preparing carvedilol, as well as a new crystalline hydrate and solvate and forms of carvedilol, processes for the manufacture thereof, and pharmaceutical compositions thereof.
CA2186784C The use of carboxylic acid derivatives as drugs The invention concerns the use of carboxylic acid derivatives of formula I (I) in which R means a formyl group, a CO2H group or a residue which can be hydrolysed to form COOH; X means nitrogen or CR14, wherein R14 means hydrogen or, together with R3, forms a 3- to 4-member alkylene or alkenylene chain in each of which a methyl group can be replaced by oxygen; Y means sulphur or oxygen or a single bond; Z means sulphur or oxygen; and the other substituents have the meanings given in the description. These derivatives can be used for preparing medicaments.
CN102125546A Composition for preventing kidney stone The invention discloses a composition for preventing kidney stone, comprising the following components in parts by weight: 10-70 parts of daidzin, 3-25 parts of genistin, 5-35 parts of glycitin, 0.1-2 parts of daidzein, 0.005-0.05 part of genistein and 0.01-0.1 part of glycitein. The total amount of the components accounts for above 80w/w% of the total weight of the composition.
CA2289206C Efficient enantioselective addition reaction using an organozinc reagent An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.
WO2012005299A1 Ros tyrosine kinase inhibitor Disclosed is a ROS tyrosine kinase inhibitor containing as an active ingredient the compound represented in general formula [1], in which either (I) or (II) hold, or a pharmaceutically acceptable salt thereof. (I) X represents CH or N, R1 represents a halogen, R2 represents a halogen, H, cyano, a group represented by general formula [9], an optionally substituted heteroaryl, etc., R3 represents H or a hydroxy, R4 represents H or an alkyl, and R5 represents H or an alkyl. (II) X represents -CRA, RA represents -CORB, RB represents an optionally substituted amino, an alkoxy or a saturated cyclic amino group, R1 represents a halogen, R2 represents H, R3 represents H or a hydroxy, R4 represents H or an alkyl, and R5 represents H or an alkyl.
CN101129355B Lovastatin sustained-release tablets and method of producing the same The invention discloses a Luovastatin slow release tablet and making method in the drug agent domain, which comprises the following parts per 1000g: 5-80g Luovastatin, 8-128g frame material, 56-896g filler, 7. 5-120mg anti-oxidant, 31-496ml binder alcohol solution with content at 0. 25%-16% and 0. 7-11. 2g lubricant. The invention has good accumulated releasing effect with good curative effect for irregular diet patients, which is beneficial for diabetic patient with little side effect.
CN101822770A Medicinal composition with anti-tumor effect and application thereof The invention discloses a medicinal composition with anti-tumor effect and application thereof. The medicinal composition uses kuh-seng alkaloid and rhizoma hterosmilacis as raw materials, and effective ingredients of the raw materials comprise matrine, oxidized matrine, sophocarpine, oxidized sophocarpine and rhizoma hterosmilacis glycoside and the like. Pharmacodynamical experiments show that the medicinal composition can be used for resisting tumor and relieving cancer swelling pain, has synergy and detoxification effects on tumor chemotherapy medicaments and effects of improving the immunity and improving the quality of life for cancer patients, and can be used for treatment of hepatitis resistance and liver fibrosis.
CN101433617A Disinfecting paste for dissolving wart and eliminating wart The invention relates to cream for dissolving wart, relieving neoplasm and detoxicating, which comprises the following components by weight portion: 0 to 3.0 portions of licorice, 0 to 3.0 portions of scutellaria, 0 to 3.0 portions of phellodendron amurense, 0 to 3.0 portions of rhubarb, 0 to 1.0 portion of menthol, 2 to 60 portions of sodium hydroxide (or potassium hydroxide), 0 to 10 portions of calcium hydroxide, and 0.75 to 1.0 portion of levobupivacaine hydrochloric acid (or toad venom, bupivacaine hydrochloric acid, lidocaine, dicaine or procaine or other local anesthetics). The sodium hydroxide (or the potassium hydroxide) and the calcium hydroxide of proper concentration can quickly dissolve protein, and melt the wart, the neoplasm and various inflammatory tissues in time from 1 minute to tens of minutes; the scutellaria, the phellodendron amurense and the rhubarb resist bacteria and virus; the licorice and the scutellaria adjust immune function, and inhibit adverse tissue reaction; the toad venom has anti-inflammatory, anti-cancer and local anesthetic functions; the menthol is fresh and cool, and can deodorize and stop pain; and the levobupivacaine hydrochloric acid or other local anesthetics has local anesthetic and paregoric functions.
US20090203628 Composition, Method And Kit For Treating Skin Disorders And Improving Skin Condition The present invention provides a composition, method and kit for treating skin disorders and improving skin condition. The composition, method and kit is particularly suited for treating acne vulgaris, seborrhea, rosacea, hirsutism, psoriasis, oily skin, dry skin, discoloration, post inflammatory hyper pigmentation, sun spots, and wrinkles.
CN102178651B Tretinoin fat emulsion injection and preparation method thereof The invention discloses a tretinoin fat emulsion injection, which contains the following components: tretinoin, oil for injection, emulsifying agent, stabilizing agent, isotonic regulator and water for injection, wherein the concentrations of the components are as below: 0.02 to 10mg/ml of tretinoin, 5 to 30g/ml of oil for injection, 0.8 to 3.0g/ml of emulsifying agent, 0.1 to 2.0g/ml of stabilizing agent and 2 to 3g/ml of isotonic regulator. The fat emulsion injection of the invention has uniform appearance quality in accordance with detection, has the average particle size below 500nm and the pH from 5.0 to 9.0, and can be used for injection. The tretinoin fat emulsion injection prepared in the invention has large drug loading of long circulating preparation, good stability and simple and feasible preparation process, and can be used for the treatment of acute promyelocytic leukemia as well as cancers, such as liver cancer, lung cancer, mammary cancer, skin cancer, cervical carcinoma, central nervous system tumors and the like. The tretinoin fat emulsion injection is expected to become the new tretinoin preparation for clinical administration.
EP2324838A1 Compositions Comprising Dimethyl Sulfoxide (DMSO) The invention relates generally to compositions comprising dimethylsulfoxide (DMSO) and associated compounds in combination with one or more of the following: fructose 1,6-diphosphate, L-arginine, L-lysine, L-aspartate, and urea. Methods for treating traumatic brain injury, ischemic stroke, atherosclerosis, spinal cord trauma, and neurodegenerative illnesses are also provided.
US20100113466 Oxazole-pyridazine-oxazole alpha-helix mimetic There are provided alpha helix scaffolds mimicking i, i+3/i+4, i+7 or i+11 residues having the general structure oxazole-pyridazine-piperidine or oxazole-pyridazine-oxazole. The common pyridazine heterocycle originates from substituted or unsubstituted dimethyl 1,2,4,5-tetrazine-3,6-dicarboxylate. These scaffolds are synthetic counterparts of amphiphilic alpha helices having a hydrophilic face along one side and a hydrophobic face along the other side of the helix.
WO2008144072A1 Dose forms comprising vx- 950 and their dosage regimen The present invention relates to antiviral therapies and compositions for treating or preventing Hepatitis C infections in patients and relates to other methods disclosed herein. The invention also relates to kits and pharmaceutical packs comprising compositions and dosage forms. The invention also relates to processes for preparing these compositions, dosages, kits, and packs.
US20090105184 Positron emission tomography probes for imaging immune activation and selected cancers Compounds for use as PET probes and methods for synthesizing and using these, comprising [18F]D-FAC and other cytosine and adenosine analogs.
US7763632 administering drugs succh as N-[2-diethylamino-5-{N-ethyl-N-(trifluoroacetyl)amino}pyrimidin-4-yl]-L-4'-{(pyrrolidin-1-yl) carbonyloxy}phenylalanine, for the treament asthma, multiple sclerosis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, graft versus host disease and arthritis Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
WO2010048788A1 A ophthalmic flurbiprofen ester nano-emulsion in-situ gel formulation and the preparation method thereof A ophthalmic flurbiprofen ester nano-emulsion in-situ gel formulation and the preparation method thereof is disclosed. The formulation comprises flurbiprofen ester, oils, emulsifying agent, thickening agent, osmotic pressure modifier, bacteriostatic agent, pH regulator, and purified water.The formulation further comprise metal chelating agents. The emulsifying agent is chosen from lecithin, polysorbate, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, and their mixtures. The thickening agent is ion-sensitive polymer and chosen from, for example gellan gum, sodium alginate and carbomer. The metal chelating agent is chosen from EDTA, EDTA-2Na, EDTA-Ca, EDTA-2K and their mixtures.
EP1296679B1 Dermal therapeutic system containing non-steroidal antiphlogistics with selective cox-2 inhibition The invention relates to a dermal therapeutic system which enables a COX-2 inhibitor to be continuously supplied to the skin and the adjacent articular structures over a long period of time. Said dermal therapeutic system can either be a transdermal therapeutic system (TTS) or a superficial therapeutic system (STS).
WO2012108622A1 Composition for preventing or treating obesity, dyslipidemia, fatty liver or diabetes containing indole-3-carbinol derivative as active ingredient Disclosed is a composition for preventing or treating obesity, dyslipidemia, fatty liver or diabetes, containing an indole-3-carbinol derivative as an active ingredient. The indole-3-carbinol derivative of the present disclosure can be usefully used as a pharmaceutical or functional food composition for preventing or treating obesity, dyslipidemia, fatty liver or diabetes by inhibiting differentiation of preadipocytes and reducing accumulation of triglyceride in cells.
US20100144719 Pharmaceutical suspension The present invention is directed to the provision of a pharmaceutical suspension. The suspension includes high molecular weight polyethylene glycol as a suspending agent. The suspension also typically includes an antimicrobial agent (e.g., polymeric quaternary ammonium compound), an antimicrobial system (e.g., borate/polyol complex system) or both. The suspension has been found particularly useful as an ophthalmic suspension, but can be used in other instances as well.
CN103083278A Roxithromycin capsule and preparation method thereof The invention discloses a roxithromycin capsule and a preparation method thereof. The roxithromycin capsule pharmaceutical composition comprises the roxithromycin, silica powder, a disintegrating agent, a filler, a lubricant, etc. The preparation technology of the roxithromycin capsule comprises a direct filling technology and a wet granulation process. The method can satisfy demands of different equipment and is beneficial for production. The prepared roxithromycin capsule is good in dissolution and small in loading difference, and is a safe, stable and effective product.
WO2006013904A1 Medicinal composition containing meltrin antagonist Mainly concerning the pharmaceutical field, it is intended to exert an inhibitory effect on the function of meltrin α of promoting the differentiation of adipocytes by preparing a compound serving as an antagonist to meltrin α (for example, an antisense inhibiting the expression of a meltrin α gene or an anti-meltrin α antibody capable of inhibiting the physiological activity of meltrin α) and administering the same. By employing such a meltrin α antagonist as described above as the active ingredient, it becomes possible to provide a preventive/remedy which is efficacious against fatness, obesity or various diseases caused by obesity or relating thereto such as diabetes.
US7332492 Amino substituted dibenzothiophene derivatives for the treatment of disorders mediated by NP Y5 receptor Compounds of formula (I): wherein: X is a group of formula (B): and R1, R2, R4, n, x, y and z are as defined within are described. Processes for their preparation and their use in the treatment of disorders mediated by the neuropeptide Y5 receptor in a warm-blooded animal, such as a human being, are also described.
EP1442022A4 Polyamide modulators of cox2 transcription Processes and compositions are provided for regulating COX2 gene expression in a cell. The process includes selecting a polyamide composition comprising N-methyl pyrrole (Py) and N-methyl imidazole (Im) to provide specific binding to DNA at a COX2 gene target site in a cell. The polyamide is then combined with the cell containing the COX2 gene, wherein the polyamide binds to the COX2 gene promoter target site and regulates transcription of the COX2 gene.
CN101011484B Medicine for treating urinary system infection disease and preparation method of its capsule The invention relates to a method for preparing the drug and relative capsule used to treat urinary system infection. The inventive drug is formed by phellodendron bark, Cape jasmine, Chinese pink herb, licorice, French chalk or the like, as material. And the preparation comprises that boiling phellodendron bark in water, depressurizing and concentrating into paste, adding alcohol, laying, recycling the alcohol and obtaining the concentrated dense paste, boiling Cape jasmine, Chinese pink herb, licorice or the like in water, depressurizing and concentrating to obtain the clear paste, adding alcohol, laying, recycling the alcohol and obtaining the concentrated dense paste; combining two dense pastes, adding French chalk powder, mixing uniformly, depressurizing, drying and breaking into powder, packing into capsule. The invention has more than 80% effect on 30 clinical samples, for treating urinary system infection.
US20080248044 Polyepitopic protein fragments of the e6 and e7 proteins of hpv, their production and their use particularly in vaccination Polyepitopic peptides of E6 and E7 proteins of Human Papillomavirus, their production, and methods of treating pathologies in which a polyepitopic peptide of the E6 and E7 protein of Human Papillomavirus is recognized by the cellular immune system.
US20120238514 Novel crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use The invention relates to crystalline hydrates of the formula I in which n has a value of from 2.1 to 2.5. The compound is suitable, for example, as an antidiabetic.
EP1119361A4 Treatment of carcinomas using squalamine in combination with other anti-cancer agents or modalities A method for treating a tumor includes a first treatment procedure using a conventional cancer treatment technique, and a second treatment procedure which includes administering an effective amount of squalamine. Synergistically effective amounts are preferred. The first treatment procedure may be a treatment with one or more conventional cytotoxic chemical compounds. As examples, the cytotoxic chemical compound may be a nitrosourea (such as BCNU), cyclophosphamide, doxorubicin, 5-fluorouracil, paclitaxel and its derivatives, cisplatin or other platinum containing cancer treating agents. Alternatively, the first treatment may be a treatment with one or more conventional anti-hormonal agents. As examples, the anti-hormonal agents may be a LHRH (luteinizing hormone releasing hormone) agonist or an anti-androgen such as flutamide, biclutamide, nilutamide, and luprolide. These conventional cancer treatments compounds and the squalamine may be administered by any suitable route. The first treatment procedure may take place prior to the second treatment procedure, after the second treatment procedure, or the two treatment procedures may take place simultaneously. As an alternative, the first treatment procedure may be a conventional radiation treatment regimen. As a further alternative the first treatment procedure may be a combination of treatment with one or more conventional cytotoxic chemical compounds and a conventional radiation treatment regimen.
CN102302636A Medicament for treating burn and preparation method thereof The invention discloses a medicament for treating burn. The medicament is prepared from dragon's blood, Chinese angelica, kaolin, calamine, pearl, rhinoceros horn, frankincense, musk, myrrh, paris root, realgar, watermelon frost, prepared elephant hide, borax, dicatechin, borneol and gypsum rubrum which serve as raw materials. The medicament can be prepared into various medicines which are used clinically. In a formula, the medicaments are reasonable in compatibility, have the effects of clearing heat and detoxicating, inducing diuresis, relieving pain and stopping bleeding and promoting tissue regeneration under the synergetic treatment action, and are suitable for burn symptoms of different degrees. Clinical test results prove that the medicament has an obvious effect, does not have toxic or side effect, and is safe and reliable in clinical application.
US20090209636 Novel use of (-)-epigallocatechin gallate An apparatus for generating a data stream having a series of segments using data organized in subsequent data frames, a data frame having more important and less important data. It comprises a packetiser for packetising data from a data frame into the series of segments having a first segment and a second segment, where the packetiser is operative to packetise the data of the frame so that a starting point of the more important data coincides with a starting point of the first segment and an information block adder for adding a first information block to the first segment.
CN102048858A Medicine composition for treating cirrhosis, hepatic ascites and liver cancer The invention provides a Chinese material medical preparation comprising total saponin of American ginseng, tanshinone II a, total saponin of the root of Chinese thorowax, total lignan of the fruit of Chinese magnoliavine, giant knot weed alcohol extract, oldenlandia diffusa alcohol extract, bear gall and ovelecithin. The Chinese material medical preparation is used for treating cirrhosis, hepatic ascites and liver cancer. The Chinese material medical preparation is used for treating cirrhosis and hepatic ascites with cure rate reaching 80 percent and effective rate reaching 95 percent through strengthening the body resistance, tonifying qi and yin, promoting blood circulation and removing blood stasis, clearing heat and detoxicating, inhibiting tumors and resisting hepatic fibrosis, and treating the liver cancer with cure rate reaching 60 percent and effective rate reaching 80 percent.
DE102005060377A1 Composition, useful for preparing compressed form, preferably tablets to treat senile dementia, preferably for preventing and alleviating Alzheimer's disease, comprises donepezil hydrochloride of polymorph form Composition for the preparation of compressed form, preferably tablets, comprises donepezil hydrochloride of the polymorph form (I), where the composition is injected directly. Independent claims are included for: (1) a method for preparing compressed form containing (I), comprising directly injecting the composition; and (2) a compressed form, obtained by the above method. - ACTIVITY : Nootropic; Neuroprotective. - MECHANISM OF ACTION : Acetylcholine esterase inhibitor.
WO2005027888A1 Use of the effective constituents from rhubarb for the manufacture of a medicament for the enhancement of as2 o3 induced apoptosis This invention relates to the use of the effective constituents from Rhubarb for the manufacture of a medicament for the enhancement of arsenic trioxide (As203) induced apoptosis. The effective constituents from Rhubarb are anthraquinone compounds of formula I separated and purified from natural plant Rheum, or the extracts including the effective constituents extracted from Rhubarb by means of chemical solvents. Formula I. It is proved that the effective constituents from Rhubarb enhance the susceptibility of tumor cells to As203-induced apoptosis through elevating cellular reactive oxygen species (ROS) level by experimental study in vivo and in vitro. This invention also relates to pharmaceutical preparations comprising the effective constituents from Rhubarb alone or in combination with As203, which enhance As203-induced apoptosis, control the dose of As203, relieve the toxicity and side-effect caused by As203, and expand the chemotherapy spectrum of As203.
EP2100615A1 Cancer therapy The present disclosure provides methods for treating a cancer patient. The methods rely on the observation that cells of the immune system which target a tumour cell ("effector cells") clonally expand before a population of "regulator" or "suppressor" cells which down-regulate the activity of the immune cells which target the tumour cell. Methods are provided herein which stimulate effector cell production and also provides means for inhibiting the production of, limiting the function of, and/or destroying, regulator cells, in the treatment of cancer.
CN101912492A Bitongling tincture The invention discloses a bitongling tincture and relates to a Chinese patent medicament for treating arthralgia due to wind-dampness and sprain. The medicament consists of Chinese angelica (alcohol-washed), suberect spatholobus stem, szechuan lovage rhizome, eupolyphaga, crude myrrh, crude frankincense, Chinese wild ginger, tuberculate speranskia herb (fried), clematis root, impatiens balsamina L, honeysuckle flower, angelica dahurica (fried), dandelion, philippine violet herb, hindu datura flower, cloves, goat bone, mulberry twig, mint, wild pepper, flos inulae, cassia bark, kadsura coccinea (Lem.) A. C. Smith, ant, camphor and bscured homalomena rhizome. The bitongling tincture is prepared by the following steps of: infusing raw materials, chopping the infused raw materials and drying; grinding the dried raw materials into powder; putting the powder into a container; adding edible alcohol and purified water into the container; uniformly stirring the mixture once every 1 to 2 days; sealing the container at any time; soaking the mixture for 30 days; opening the container; removing residues by filtering to obtain liquid bitongling tincture; and bottling the liquid bitongling tincture for later use. The bitongling tincture is applied externally to effectively treat osteoarthrosis, rheumatic (rheumatoid) arthritis, cervical spondylosis, protrusion of lumbar vertebral disc, ankylosing spondylitis, scapulohumeral periarthritis, sprain, skin eruptions (including diabetic foot), mastitis (hyperplasia), prostatitis (hyperplasia), chronic cholecystitis, osteoproliferation, mosquito bite and the like.
EP2699581A1 2-oxo-1-imidazolidinyl imidazothiadiazole derivatives The present invention relates to 2-oxo-1-imidazolidinyl imidazothiadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
CN102558190A (R)-N-brooethyl naltrexone crystal form compound and preparation method, combination and application thereof The invention discloses an (R)-N-brooethyl naltrexone crystal form compound. An X-ray diffraction pattern of the crystal form compound comprises an X-ray diffraction maximum shown as the following 2 theta: 15.86 degrees +/- 0.2 degree and 25.60 degrees +/- 0.2 degree. In addition, a preparation method of the crystal form compound and the application of the crystal compound to preparation of medicine, particularly medicine for treating side effects caused by opioid substances are further disclosed. A medicine combination containing the crystal form compound and the application of the medicine combination are further disclosed.
US8105579 Bacteriophage-containing therapeutic agents The present invention relates in its broadest aspect to combined phage/antibiotic therapy. More particularly, it relates to use of (i) one or more bacteriophages and (ii) one or more antibiotics in the manufacture of a combined product for simultaneous, separate or sequential administration of (i) and (ii) to treat a bacterial infection characterized by biofilm formation, for example an infection comprising or consisting of P. aeruginosa. Treatment in this context may be either therapeutic or prophylactic treatment. Also provided are deposited bacteriophages each exhibiting different strain specificity against P. aeruginosa and combinations of such bacteriophages, e.g. a panel of six deposited bacteriophages which was found to be effective against a high percentage of clinical isolates of P. aeruginosa from canine ear infections.
CN102961371A Ibuprofen arginine granule and preparation method thereof The invention relates to an ibuprofen arginine granule, which is composed of ibuprofen arginine, a filler, a taste masking agent, an adhesive, a flavoring agent, a smelling agent, and a coloring agent by weight part. The invention also provides a preparation method of the ibuprofen arginine granule. The ibuprofen arginine granule provided by the invention covers up the intrinsic spicy taste of ibuprofen arginine, and has the advantages of good children compliance, fast effect, simple prescription composition, easily available and cheap auxiliary materials with fewer variety and dosage, and no need of coating. The preparation method has the characteristics of simple process, easy operation, no need for special equipment, short production cycle, and low cost, thus being suitable for industrialized production.
CN101804054A Application, preparation and preparation method of synthetic palmatine The invention discloses application and a preparation of synthetic palmatine (or inorganic salts, such as hydrochloride, sulfate, phosphate, and the like, and organic salts or derivatives) prepared by a chemical synthetic method, the preparation of raw materials and the fine preparation of raw materials. The synthetic palmatine are needle-like crystals or particle crystals of light yellow to dark yellow. Firstly proved by pharmacological and toxicological substitution research, the synthetic palmatine can be used as medicines instead of palmatine extracted from plants, has better effects than the palmatine extracted from plants in the curative effect aspects of resisting inflammation, bacteria, viruses, and the like, is synthesized by the disclosed methods or the method in the invention, can be prepared into injections, and like to be applied to clinical departments of resisting bacteria, eliminating inflammation and resisting inflection.
WO2007107598A1 Phosphorylated a2a receptor agonists A phosphorylated A2A receptor agonist providing agonist properties on the A2A receptor after dephosphorylation the phosphorylated A2A receptor agonist comprises a ribosyl moiety and a purine moiety and being phosphorylated at the 5'-position of the ribose moiety except adenosine monophosphate (AMP), adenosine diphosphate (ADP) or adenosine triphosphate (ATP), a medicament containing the compound of the invention including ADP and the use of the compound of the invention including ATP and ADP for several medical indications e. g. inflammatory events. In particular, compounds of formula (I) are also disclosed.
US7452904 1-alkyl-1-azoniabicyclo' 2.2.2 octane carbamate derivatives and their use as muscarinic receptor antagonists Carbamate of general formula (I), wherein R1, R2, and R3 are H, OH, NO2, SH, CN, F, Cl, Br, I, COOH, CONH2, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylsulfanyl, (C1-C4)-alkylsulfinyl, (C1-C4)-alkylsulfonyl, (C1-C4)-alkoxyl optionally substituted with one or several F, and (C1-C4)-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C5-C10)-alkyl, a substituted (C1-C10)-alkyl; and X− is a physiologically acceptable anion. Carbamate (I) is selective M3 receptor antagonists versus M2 receptor and may be used for the treatment of urinary incontinence (particularly, the one caused by overactive bladder), irritable bowel syndrome, and respiratory disorders (particularly, chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema, and rhinitis), as well as in ophthalmic interventions.
WO2012130893A1 Use of epigallocatechin gallate as an antiviral agent against infections by the hepatitis c virus The present invention relates to a flavonoid compound of formula I, where R3, R5 and/or R7 is a group of formula II, or R1 and R2 are both OH groups, or to one of the pharmaceutically acceptable salts or esters thereof, for use as an antiviral agent in the treatment and/or prevention of a hepatitis C virus (HCV) infection. The invention also relates to an ex vivo method for reducing the infectivity of HCV or for inactivating HCV, including a step of contacting said hepatitis C virus with a compound of formula (I).
WO2007090289A1 Combinations of botanical extracts for promoting cardiovascular health A blood lipid lowering agent that functions through a same mechanism as berberine (e.g. berberine, one or more pharmacologically acceptable salts of berberine or a mixture thereof) and a blood lipid lowering agent that functions through a different mechanism than berberine (e.g. phytosterols, phytostanols, esters thereof or mixtures thereof) act synergistically to improve blood lipid profiles, for example, lowering total cholesterol, LDL-C or nonHDL-C, and triglyceride, and increasing the ratio of HDL-C to nonHDL-C. The two may be used in combination to treat or reduce the chance of contracting cardiovascular disease, hyperlipidemia, atherosclerosis, coronary heart disease, angina, cerebrovascular disease, stroke, overweight or obesity, diabetes, insulin resistance, hyperglycemia, hypertension, arrhythmia, diseases of the central nervous system, diseases of the peripheral nervous system and/or inflammation. The blood lipid lowering agent that functions through a same mechanism as berberine, with or without the blood lipid lowering agent that functions through a different mechanism than berberine, may also be used to control weight.
US20100267670 Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms) The present invention is directed to novel heterocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
CN103285013A Medical composition for preventing and treating pneumonia disease of cattle and hogs and preparation method thereof The invention discloses a medical composition for preventing and treating pneumonia disease of cattle and hogs and a preparation method thereof. The medical composition based on 1000ml of liquid medicine comprises medicines and auxiliary materials: 250-350g of florfenicol, 2-8g of meloxicam, 40-80ml of 1, 2-propylene glycol, 80-250ml of 2-pyrrolidone, 650-900ml of polyethylene glycol-400 and 10-15ml of benzyl alcohol. The preparation method comprises the following steps: preparing a mixed solvent; primarily preparing a liquid medicine; preparing an injection. Massive clinical application verifies that the medicine has anti-microbial, anti-inflammatory and anti-mycoplasma functions and has the characteristics of high and long effects to treat and prevent infectious diseases of the upper respiratory tract of cattle and hogs, especially various pneumonia diseases including mycoplasma pneumonia syndrome. The medical composition is good in treatment effect, and has a positive effect to drive development of cattle and hog raising industry in China.
US6992075 dehydrogenating estrogenic salts by heating in high humidity to produce conjugated estrogen salts; 14-hydroxy (or hydroperoxy)- Delta 8,9-Dehydroestrone Sodium Sulfate; side effect reduction; hormone replacement therapy The present invention relates to novel estrogenic compounds. The present invention also relates to methods of treating estrogen deprivation in a subject comprising administering novel estrogenic compounds. Additionally, the present invention relates to methods of synthesizing novel estrogenic compounds.
WO2014007549A3 Composition for preventing or treating colitis comprising s-allyl-l-cysteine as active ingredient, and medical preparation comprising same The present invention relates to a composition for preventing or treating colitis. According to one embodiment of the present invention, the composition for preventing or treating colitis comprises S-allyl-L-cysteine, a pharmaceutically acceptable salt thereof, or a solvate or hydride of same as an active ingredient, and exhibits an anti-inflammatory (anti-inflammation) action in colitis. The composition for preventing or treating colitis has an outstanding effect in preventing and alleviating colitis due to the effect of the anti-inflammatory action and the effect of an antioxidant action of S-allyl-L-cysteine, while at the same time S-allyl-L-cysteine is not accompanied by side-effects and so has a wide scope of use against colitis.
CN102988368A High-purity texaphyrin metal complex The invention discloses a method for improving and synthesizing a texaphyrin metal complex and a composition. A high-purity texaphyrin metal complex composition is generated by the improved synthesis method, wherein about more than 98 percent of texaphyrin metal complex has the same structure and/or same molecular weight. The invention also describes a pharmaceutical composition containing the high-purity compositions and application of the high-purity compositions in treatment of cancers, cardiovascular diseases and affections.
US20080226717 Sublingual Coated Tablet The present invention relates to a sublingual coated tablet and to a method for the preparation thereof. The tablet includes a core devoid of a pharmaceutically active substance, and a coating including at least one active substance. The preferred active substance is an opioid analgesic.
CA2379581C Echinacea supplement and method of manufacture In one aspect, the present invention provides Echinacea compositions including standardized amounts of at least two Echinacea components. More preferably the Echinacea compositions of the present invention include standardized amounts of at least three Echinacea components are cichoric acid, Echinacea alkylam ides and Echinacea polysaccharides. In another aspect. the present invention provides methods for preparing Echinacea compositions, the methods including the step of combining amounts of at least two Echinacea components, preferably three Echinacea components, sufficient to yield an Echinacea composition including standardized amounts of each of the combined Echinacea components. In yet another aspect, the present invention provides Echi-nacea extracts, and methods for preparing Echinacea extracts. Presently preferred Echinacea extracts are enriched in one or more members of the group consisting of polysaccharides, alkylamides and cichoric acid. In yet another aspect, the present invention provides methods for enhancing immune system activity in a mammal.
WO2009080835A1 Thyromimetric compounds in treatment of disease related to sonic hedgehog signalling This invention relates to compounds for the treatment of disease induced, caused or dependent on activation of the Sonic hedgehog pathway, wherein the compound is a thyromimetic lacking inner-ring iodines. Preferably the compound is of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, formula (I), wherein G is a group selected from: formula (II) (III) (IV) (IV) and the remaining groups/substituents are as defined herein.
CN101102778A Substance mixture The invention relates to a substance mixture containing at least one glucocorticoide and at least one N-chloro compound and/or at least one O-chloro compound, in addition to at least one medicament which contains said type of substance mixture. The invention also relates to the use and production of said type of medicament for the topical treatment of inflammations.
CN1723955A Extractive of rhizome belamcandae, prepn. method and use thereof A extract series of belamcanda rhizome, including the flavone, flvonoside and flavone aglycon of belamcanda, its extracting process and its application in preparing the medicines for preventing and treating the diseases in respiratory system are disclosed.
CN102641502A Novel use of aromatase inhibitors The invention relates to a novel use of aromatase inhibitors, in particular to application of the aromatase inhibitors in terms of preparation of medicines for treating male bladder outlet obstruction and lower urethral syndromes caused by the same. The medicines can rapidly and effectively treat bladder outlet obstruction of male mice. The novel use can be clinically applied better, provides a fundamental basis for clinical treatment, and is a novel method for treating the bladder outlet obstruction.
WO2008090286A3 Derivatives of imidazo, pyrimido and diazepine pyrimidine-dione, and use thereof as a drug The present invention relates to new derivatives of imidazo, pyrimido and diazepine-pyrimidine-dione of the general formula (I) in which R1, R2, L1, L2, Y, Z and A are various and varying groups. These products exhibit a good affinity for certain sub-types of cannabinoid receptors, in particular the CB2 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more cannabinoid receptors are involved. The invention also relates to pharmaceutical compositions containing said products, and to the use thereof for preparing a drug.
CN101869544A Ambroxol hydrochloride controlled release suspension and preparation method thereof The invention discloses controlled release suspension of ambroxol hydrochloride which is controlled to release in a gastrointestinal tract environment. The preparation contains the ambroxol hydrochloride and pharmaceutically acceptable polymer. The suspension comprises the following components in percentage by weight: 10 to 90 percent of ambroxol hydrochloride and 10 to 90 percent of auxiliary material. The auxiliary material having the controlled-release effect is of one or more of cation exchange resin, methylcellulose, ethylcellulose, acrylic resin and Hydroxypropylmethyl Cellulose. Compared with the rapid-release preparation, the suspension can maintain the valid blood concentration within 24 hours, can improve the treatment effect, has small toxic and side effect, is convenient to take and carry, and can reduce the taking times. Compared with the slow-release preparation, the suspension can maintain more stable blood concentration within 24 hours, can improve the treatment effect, and has small toxic and side effect. The suspension is only required to be taken one time every day. The suspension is used as phlegm medicine clinically.
CN102101858A Preparation method of ramosetron derivatives and applications thereof The invention relates to a preparation method of ramosetron derivatives and applications thereof. The invention provides a compound as expressed in the formula (I), a pharmaceutically acceptable salt thereof, an enantiomer or racemic mixture thereof, wherein, R1 is H, C1-C6 alkyl, C1-4 alkyloxys, aryls or substituted C1-C4 alkyl. The invention also provides a preparation method of the compound or the pharmaceutically acceptable salt thereof, the pharmaceutical composition containing the compound and the salt, and applications of the compound. The compound in the invention possesses functions of preventing and treating the digestive tract symptoms of nausea, vomit, etc. caused by anti-malignant tumor treatment, and preventing and treating irritable bowel syndrome. The compound can be used in preparing medicine for preventing and treating the digestive tract symptoms of nausea, vomit, etc. caused by anti-malignant tumor treatment, and irritable bowel syndrome.
US20120252864 Substituted isoindoline-1,3-dione derivatives This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.
US20090012018 Inhibition of pancretic cancer cell growth The present invention relates to compositions and methods for inhibition of signal transduction pathways in cancer cells. In particular, the present invention provides methods and compositions comprising Wnt and Hedgehog pathway inhibitors for reducing proliferation of adenocarcinoma cells.
WO2009110526A1 Prophylactic or therapeutic agent for optic nerve disorders comprising 3',5-di-2-propenyl-(1,1'-biphenyl)-2,4'-diol as active ingredient Disclosed is a compound which is useful as a prophylactic or therapeutic agent for optical nerve disorders, an inhibitor of the cell death of retinal ganglion cells or an agent for recovering the expression level of a neurofilament light chain, particularly a compound which can exhibit the above-mentioned physiological activity when administered orally. Specifically disclosed is 3'-5-di-2-propenyl- (1,1'-biphenyl)-2,4'-diol, an ester thereof, or a salt of the compound or the ester. The compound, the ester or the salt can significantly prevent the reduction in the number of cells in a retinal ganglion cell layer in an NMDA-induced retinal disorder model rat when administered orally to the model rat and can recover the reduction in the expression level of a neurofilament light chain in a retina in the model rat when administered intravitreally to the model rat. Therefore, the compound, the ester or the salt is useful as a prophylactic or therapeutic agent for optical nerve disorders, an inhibitor of the cell death of retinal ganglion cells or an agent for recovering the expression level of a neurofilament light chain.
EP1259481B1 Substituted benzoylguanidines, method for their production, their use as a medicament or diagnostic agent and a medicament containing the same The invention relates to benzoylguanidines of formula (I), wherein R2 stands for -Y-p-(C6H4)-R11, -Y-m-(C6-H4)-R11 or -Y-o-(C6H4)-R11; R11 represents (C1-C9)-heteroaryl, which is bonded by C or N and is substituted or unsubstituted with 1 to 3 substituents selected from the group consisting of F, Cl, CF3, CH3, methoxy, hydroxy, amino, methylamino, dimethylamino and benzyl; Y represents oxygen, -S- or NR12; R12 represents H or (C1-C4)-alkyl; R4 F, Cl, Br, I or C1-C4-alkyl; R1 and R3 are defined as per the claims. Said benzoylguanidines are suitable for use as anti-arrhythmic medicaments containing cardioprotective components for the prophylaxis and treatment of infarcts and for the treatment of angina pectoris. They also preventively inhibit the pathophysiological processes associated with the origination of defects caused by ischaemia, in particular during the triggering of ischaemically induced cardiac arrhythmia.
US7396663 Isolated polynucleotide encoding a G-protein coupled receptor The invention provides human G-protein coupled receptors (GCREC) and polynucleotides which identify and encode GCREC. The invention also provides expression vectors, host, cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating, or preventing disorders associated with aberrant expression of GCREC.
WO2013190509A3 Preparation of intermediates of boceprevir Processes for preparing intermediates of Boceprevir and their use in preparation of Boceprevir or its pharmaceutically acceptable salts are provided.
US6949583 Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method of preparing same and compositions containing same The invention relates to benzofuran or benzothiophene derivatives, to processes for preparing them, to pharmaceutical compositions comprising them, and to the method of use thereof in the treatment of pathological syndromes of the cardiovascular system.
CN101347623A Multifunctional nanodevice platform The present invention relates to novel therapeutic and diagnostic arrays. More particularly, the present invention is directed to dendrimer based multifuntional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems generally comprise two or more separate components for targeting, imaging, sensing, and/or triggering release of a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
CN102389437A Application of Centella triterpenes in preparing products for improving cerebral apoplexy sequelae The invention relates to the application of Centella triterpenes in preparing products for improving cerebral apoplexy sequelae, in particular to the new use of Centella asiatica alpha-amyrin triterpenes (including asiaticoside, asiatic acid, hydroxyl asiaticoside and madecassic acid) in preparing products for improving cerebral apoplexy sequelae. The animal studies prove that asiaticoside, asiatic acid, hydroxyl asiaticoside and madecassic acid show significant bioactivities and strong pharmacological actions and can be used for treating cerebral apoplexy sequelae, such as depression, dementia (vascular dementia) and limb disorders. The Centella triterpenes are advantageous in stable property, abundant raw material resources, low price, high safety and low toxicity, provide a new drug resource for prevention, diagnosis, detection, protection, therapy and research of cerebral apoplexy sequelae, have a simple preparation process and a high yield, are suitable for industrial, and are significant in development and utilization of medicinal plant resources in China.
US7109296 Used to identify modulators of the 5-HT3 serotonin receptor complex, and to reconstitute a more realistic physiological 5-HT3 receptor response in recombinant systems DNA encoding human 5-HT3-C has been cloned and characterized. The recombinant protein is capable of forming biologically active human 5-HT3-C protein. The cDNA has been expressed in recombinant host cells that produce active recombinant protein. In addition, the recombinant host cells are utilized to establish a method for identifying modulators of the receptor activity, and receptor modulators are identified.
CN102488676A Application of teprenone in preparing medicine used for preventing and/or treating depression The invention discloses an application of teprenone in preparing a medicine used for preventing and/or treating depression. The invention belongs to the technical field of medicines. According to the invention, as a result of experiments, teprenone can protect nerve cells from the poisoning of dexamethasone, and assists in resisting mice disappointment behaviors. With teprenone, mice swim motionless time and mice tail suspension motionless time are substantially reduced. Teprenone is advantaged in substantial treatment effect, high safety, and low cost.
US20120009168 Improved emulsifying system for nutraceutical compositions The inventive composition allows the solubilization of hydrophobic nutraceuticals in water to produce clear and stable solutions. The hydrophobic nutraceutical is combined with a lecithin and optionally other components to form an oil. Sucrose is dissolved in water and combined with hydrophilic cosolvents. Sucrose fatty acid ester emulsifier is dissolved in the sucrose-cosolvent mixture. The nutraceutical oil is homogenized into the sucrose ester emulsifier solution to form a stable homogenate that can be readily dispersed into an aqueous solution.
WO2013166413A2 Compositions and methods for increasing neurotrophic peptides A pharmaceutical composition is provided which includes a pharmaceutically acceptable excipient and a pharmaceutically and physically acceptable amount of a compound selected from the group consisting of Chemical Formulas I-IV as described herein, or a pharmaceutically acceptable salt thereof. Also provided are methods of increasing a level of a defined neurotrophic peptide in an organism or tissue comprising the administration of a pharmaceutically and physically acceptable amount of one or more of the compositions described above, and a method for treating a neurodegenerative disease in a subject in need thereof, the method comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 1.
CN102920932A Medicinal composition for treating eczema The invention relates to a medicinal composition for treating eczema. The medicinal composition is characterized in that the medicinal composition is an ointment prepared from 250-350 parts by weight of mature red sorghum, 25-35 parts by weight of Boswellia carteri, 25-35 parts by weight of myrrh and 2-4 parts by weight of borneol. The preparation method of the ointment comprises the following steps: carbonizing by stir-frying the mature red sorghum, grinding to obtain powdery mature red sorghum for later use, co-grinding the Boswellia carteri, the myrrh and the borneol to form fine powder, adding the fine powder to the powdery mature red sorghum, uniformly mixing, and adding Chinese prickly ash oil to prepare the ointment. The use method of the ointment comprises the following steps: uniformly applying a proper amount of the ointment on an infected part once everyday, and continuously using for three days. The medicinal composition has the advantages of simple and resultant compatibility, use convenience, and substantial curative effect.
US8772311 Harmine derivatives, intermediates used in their preparations, preparation processes and use thereof This invention relates to compounds of general formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the specification; intermediates used in their preparation, preparation processes and use thereof. The present invention produces new harmine derivatives with enhanced antitumor activity and lower nervous system toxicity by structurally modification of the parent structure of β-carboline of harmines at position 1, 2, 3, 7 and 9. The compounds of the present invention can be prepared easily with high yield. They can be used in manufacture of a variety of antitumor medicines and medicines used in treatment of tumor diseases in combination of light or radiation therapy.
WO2007095850A1 A pharmaceutical composition of docetaxel, preparation and use A pharmaceutical composition of docetaxel comprising effective amount of docetaxel, Tween and cosolvents, wherein the cosolvent is at least one member selected from the group consisting of glycerol and polyethylene glycol. The composition is an injectable solution or a freeze-dried injectable powder. The solubility of docetaxel is improved by adding Tween and cosolvents. The preparation of the pharmaceutical composition is also disclosed.
CN101810586A L-dopa methyl ester sustained-release microsphere composite and preparation method thereof The invention discloses an L-dopa methyl ester sustained-release microsphere composite and a preparation method thereof, which belong to the technical field of medicament preparation. The L-dopa methyl ester sustained-release microsphere composite comprises the following components in percentage by weight: 50 to 99 percent of one or mixtures of polylactic acid-glycollic acid, polylactic acid and polycaprolactone and 1 to 50 percent of L-dopa methyl ester. In the invention, L-dopa methyl ester particles are prepared first and then the L-dopa methyl ester release microsphere composite is prepared by oil-in-water-oil lease solids. In the invention, the L-dopa methyl ester particles are further encapsulated in a sustained-release macromolecular material in a micro-capsule form. The surfaces of prepared microspheres are smooth and round, the homogeneous degree is high, the particles are regular and not adhered; and the encapsulation rate is high, the burst release rate is low and the drug-loading rate is high.
CN1646124B Use of materials having zinc ionophoric behavior Disclosed is a method for delivering excess zinc to eukaryotic cells to inhibit the metabolism of the cell, the method comprising treating the cells with a zinc ionophoric that is capable of delivering a zinc ion across a cellular membrane wherein the minimum inhibitory concentration (MIC) of the zinc ionophoric material is less than about 500 ppm.Further disclosed is a method for delivering excess zinc to eukaryotic cells to inhibit the metabolism of the cell, the method comprising treating the cells with a zinc ionophoric material that is capable of delivering a zinc ion across a cellular membrane wherein the zinc ionophoric material is in combination with a zinc containing material and further wherein there is an increase in an intracellular zinc level by 1.5 fold more than would occurin the absence of the zinc ionophoric material.
WO2008062450A3 Crystalline polymorphs of ciclesonide The present invention discloses a novel crystalline forms of Ciclesonide of formula (I) and the process for preparation thereof. The present invention also provides a process for preparing amorphous form of Ciclesonide.
US20120016000 Method to assay phospholipid and triglyceride transfer activity of microsomal triglyceride transfer protein The present invention is directed to a method for identifying an antagonist compound of microsomal triglyceride transfer protein (MTP), wherein the antagonist at least partially inhibits triglyceride transfer activity while not significantly inhibiting phospholipids transfer activity of MTP. In particular, the present invention is directed to assays for phospholipid (PL) and triglyceride (TG) transfer activity having considerably improved sensitivity. In addition, antagonist compounds that modulate the lipid transfer activity of MTP are provided. Kits for measuring the lipid transfer activity of MTP are also provided by the present invention.
WO2010083133A1 Compositions and methods for the treatment of throat discomfort The physiological cooling agent N-ethyl-2,2-diisopropylbutanamide exhibits a surprising selectivity for throat cooling over mouth cooling, especially when consumed in the form of a confection. Methods of treating throat discomfort using N-ethyl-2,2-diisopropylbutanamide are described. Also described are various confections that incorporate N-ethyl-2,2-diisopropylbutanamide, including hard candy confections, soft candy confections, and center-filled confections.
EP1545596A2 Use of histamine h4 receptor modulators for the treatment of allergy and asthma Methods are disclosed for identifying histamine receptor modulators that affect mast cell or basophil chemotaxis, and the use of such histamine H4 receptor modulators for the prevention, treatment, induction, or other desired modulation of asthma and/or allergic responses, or diseases and/or conditions that are modulated, affected or caused by asthma or allergic responses. Also disclosed is the use of histamine H4 receptor modulators for the prevention, treatment, induction, or other desired modulation of mast cell or basophil chemotactic responses, such as migration to a particular site, or diseases and/or conditions that are modulated, affected or caused by mast cell or basophil chemotaxis.
US20120134977 Prodrugs containing albumin binding probe The present invention provides albumin-binding probes capable of reversibly linking to short-lived amino-containing drugs and non-covalently associating with albumin in-vivo, thereby converting said drugs into inactive reactivable prodrugs having prolonged lifetime in-vivo. The invention further provides conjugates of said probes with amino-containing drugs, as well as pharmaceutical compositions and uses thereof.
WO2005092383A1 Preventive/remedy for respiratory diseases It is intended to provide a compound inhibiting the activity of a protein having an amino acid sequence which is the same or substantially the same as one of the amino acid sequences represented by SEQ ID NOS:2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62 and so on, or its salt; a compound inhibiting the expression of a gene of the above protein; an antisense nucleotide containing a base sequence which is complementary or substantially complementary to the base sequence of a DNA encoding the above protein or its partial peptide or a part of the base sequence; an antibody against the above protein or its partial peptide; and so on. The above compound, antisense nucleotide, antibody and so on are usable as a preventive/remedy for respiratory diseases, etc.
CA2630717A1 Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase This invention comprises the novel compounds of formula (I) wherein R1, R2, R3 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
US20080255184 N-[3-(4-amino-7-pyridin-3-ylthieno[3,2-c]pyridin-3-yl)phenyl]-N'-[2-fluoro-5-(trifluoromethyl)phenyl]urea; lymphoma, melanoma, small cell lung , non-small cell lung, breast, colon and pancreatic cancer The present invention provides thienopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
US20080021105 Medicine Capable of Inhibiting Activation of Transcription Factor Klf5 A medicament having an action of inhibiting activation of transcription factor KLF5 and thus inhibiting vascular remodeling and arteriosclerosis, which comprises an acyclic polyprenyl compound (e.g., polyprenylcarboxylic acid such as 3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentanoic acid and the like) as an active ingredient.
CN101695482A Glipizide orally disintegrating tablet and preparation process thereof The invention relates to a glipizide orally disintegrating tablet which comprises the following ingredients in proportions by weight: 5g of glipizide, 30.64g of mannitol, 15g of microcrystalline cellulose, 9g of crospovidone, 0.06g of aspartame, 0.3g of magnesium stearate, 0.9g of 2% povidone K30 ethanol solution in percentage by weight, 8.5g of sucrose fatty acid ester and 3g of erythritol. The glipizide orally disintegrating tablet has the effects for most type 2 diabetes and can reduce fasting blood-glucose and postprandial blood glucose. Hypoglycemic medicines are required to be taken before meals, and in order to provide the convenience for a patient to take medicine under various conditions, the orally disintegrating tablet is a more ideal dosage form. The orally disintegrating tablet is characterized by being disintegrated quickly just by very little amount of water or spittle without gritty texture, is favorable in mouthfeel and easy to swallow. The optimal auxiliary materials can enable the glipizide orally disintegrating tablet to be disintegrated more quickly and considers the hardness and the friability simultaneously so as to facilitate the molding of the orally disintegrating tablet.
US20110008351 Anticomplement polypeptides of ixodes ricinus An isolated and purified polypeptide is obtained from tick salivary glands and presents more than 75% sequence identity with at least a sequence selected from the group consisting of SEQ. ID. NO. 1.
US7196107 Thia-and oxazoles and their use as ppars activators A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R1 and R2 are independently H or C1-3alkyl, m is 0–3; X1 is NH, NCH3, O, S; R3, R4 and R5 are independently H, CH3, CF3, OCH3, allyl or halogen; X2 is (CR10R11)n wherein n is 1 or 2; R10 and R11 independently represent H, fluorine or C1-16alkyl; R26 and R27 are independently H, C1-3 alkyl or R26 and R27 together with the carbon atom to which they are bonded form a 3–5 membered cycloalklyl ring. R6 and R7 independently represent H, fluorine or C1-16alkyl; R9 is C1-6alkyl or CF3; One of Y and Z is N, the other is S or O; Each R8 independently represents CF3, OCH3, CH3 or halogen; y is O, 1, 2, 3, 4, 5. Use of a compound of formula (I) for the manufacture of a medicament for the prevention or treatment of a hPPAR mediated disease or condition, such as dyslipidemia, syndrome X, heart failure, hypercholesteremia, cardiovascular disease, type II diabetes mellitus, type 1 diabetes, insulin resistance hyperlipidemia, obesity, anorexia bulimia, inflammation and anorexia nervosa
WO2008070358A3 N-cyclopropyl-hydroxyproline-based tripeptidic hepatitis c serine protease inhibitors containing an isoindole, pyrrolopyridine, pyrrolopyrimidine or pyrrolopyrazine heterocycle in the side chain The present invention provides novel compounds that mimic peptides with a C-terminal penultimate proline, such compounds being useful as protease inhibitors, particularly as inhibitors of serine proteases, and more particularly as inhibitors of the NS3 serine protease from hepatitis C virus. The compounds find utility as antiviral agents directed at hepatitis C.
US20090192227 N-Acetylcysteine Compositions and Methods for Treating Acute Exacerbations of Inflammatory Lung Disease The present invention relates to N-acetylcysteine compositions and methods for treating inflammation and redox imbalance in acute exacerbations of inflammatory lung disease.
EP2334180A1 Alleviating disorders with combining agents that increase epoxygenated fatty acids and agents that increase camp The present invention relates to compositions and methods for promoting and enhancing the analgesic, anesthetic and anticonvulsant properties of epoxygenated fatty acids, in particular, epoxy-eicosatrienoic acids ("EETs") and inhibitors of soluble epoxide hydrolase ("sEH") in the presence of elevated levels of cyclic adenosine monophosphate ("cAMP") by combining or co-administering the epoxygenated fatty acid, EET and/or inhibitor of sEH with an agent that increases intracellular levels of cAMP, e.g., a phosphodiesterase inhibitor.
EP2785715A1 Substituted pyridine derivatives as fabi inhibitors The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors. Formula(I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
CN103157112A Application of sialic acid derivatives in preparation of polyethylene glycol (PEG) lipid derivative modifying agent The invention belongs to the field of pharmaceutical preparation, in particular to the phenomenon that the speed of blood cleaning is increased be means of eliminating or weakening a polyethylene glycol (PEG) agent using sialic acid derivatives. When the PEG agent such as PEG lipidosome, PEG emulsion and PEG nanoparticles are repeatedly injected, the cleaning speed of a secondary injection agent in the blood can be greatly increased, namely, the ABC phenomenon appears. The ABC phenomenon can be eliminated and even weakened after the sialic acid derivatives are decorated on the surface of the PEG agent.
WO2014140929A1 Process for drying bendamustine hydrochloride monohydrate Wet bendamustine hydrochloride monohydrate may be dried by a two stage process wherein rapid drying is first carried out to provide a partially dried product, which is then further dried using an inert gas of controlled relative humidity to yield dry bendamustine hydrochloride monohydrate.
CN103127070A Application of Eryngiolide A in medicines rising white blood cell The invention relates to a new use of chemical compound Eryngiolide A in the pharmacy field, and relates to application of the Eryngiolide A in preparation of medicines rising white blood cell. Use of the Eryngiolide A in preparation of anti-platelet aggregation medicines is made public for the first time, the skeleton type is completely novel, and the Eryngiolide A has an unexpectedly high low white cell inhibitory activity, probability of other compounds giving any revelation for the Eryngiolide A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in preventing and curing low white cell.
US7019030 Immunotherapeutic agents Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor α, nuclear factor κB, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.
WO2009023677A1 Derivatives of 5-amino-4, 6-disubstituted indole and 5-amino-4,6-disubstituted indoline as potassium channel modulators This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.
CA2286913C Composition and methods using an eutomer Method for improving health, survival and muscle growth rate of animals, while reducing carcass fat and improving feed efficiency by administering an optically pure eutomer of an adrenergic beta-2 agonist. The invention is also directed to food compositions comprising the adrenergic beta-2 agonists.
CN102649787A (benzimidazole-2-yl)pyridine derivative and application thereof to preparation of anticoagulant medicines The invention relates to a novel (benzimidazole-2-yl)pyridine derivative and an application thereof to preparation of anticoagulant medicines. The (benzimidazole-2-yl)pyridine derivative is an ideal thrombin inhibitor, and can be used for treating and preventing or treating thrombosis and other indications including auricular fibrillation, acute coronary syndrome, acute symptomatic phlebothrombosis, cerebral arterial thrombosis and the like.
US20110196502 Methods of Using Water-Soluble Inorganic Compounds for Implants A method for controlling generation of biologically desirable voids in a composition placed in proximity to bone or other tissue in a patient by selecting at least one water-soluble inorganic material having a desired particle size and solubility, and mixing the water-soluble inorganic material with at least one poorly-water-soluble or biodegradable matrix material. The matrix material, after it is mixed with the water-soluble inorganic material, is placed into the patient in proximity to tissue so that the water-soluble inorganic material dissolves at a predetermined rate to generate biologically desirable voids in the matrix material into which bone or other tissue can then grow.
WO2005082883A3 Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline The invention pertains to substituted quinazoline and isoquinoline of formula (I) that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE-10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders. or a pharmaceutically acceptable salt, solvate or prodrug thereof.
US20130023472 Ldl quantitation and method of use The present invention features, in certain aspects, methods of promoting endocytosis of LDL with α1PI or peptides derived from α1PI. The present invention also provides methods for decreasing LDL levels in response to α1PI augmentation therapy. In preferred embodiments, the methods are suitable for a subject who is suffering from a disease or disorder selected from heart disease, atherosclerosis, hypertension, HIV infection, viral infection, bacterial infection, leukemia, a solid tumor, or autoimmune disease.
EP1278740B1 Hydroxyphenyl-piperazinyl-methyl-benzamide derivatives for the treatment of pain Compounds of general formula (I), where R1 is selected from any one of pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C¿1?-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as separate enantiomers of the compounds and salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
CN103083233A Pharmaceutical composition of paclitaxel compound The invention discloses a pharmaceutical composition of a paclitaxel compound. The composition comprises the following components: 1 part by weight of paclitaxel, 30-35 parts by weight of polyoxyethylene castor oil, 5-10 parts by weight of sodium dodecyl sulfate, 40-70 parts by weight of 95% ethanol solvent and an appropriate amount of citric acid-sodium citrate. The composition is simple in component, little in auxiliary material dosage and good in drug stability; no crystallization phenomenon occurs when the pharmaceutical composition is placed for a long time, so that the pharmaceutical composition meets the quality requirement of an injection to insoluble particles.
US20060128633 Colchinol derivatives as vascular damaging agents The invention relates to the use of compounds of formula (I): wherein X is —C(O)—, —C(S)—, —C═NOH, or —CH(R7)— wherein R7 is hydrogen, hydroxy, C1-7alkoxy, —OR8 or —NR8R9 (wherein R8 is a group —Y1R10 (wherein Y1 is a direct bond, —C(O)—, —C(S)—, —S—, —C(O)O—, —C(O)NR11—, —SO2— or —SO2NR12— (wherein R11 and R12, which may be the same or different, each independently represents hydrogen; C1-3alkyl or C1-3alkoxyC2-3alkyl) and R10 is as defined herein, R9 includes hydrogen; R11, R12 and R13 are as defined herein and are preferably methyl; R4, R5 and R6 are as defined herein with the proviso that R5 is not hydroxy, alkoxy, substituted alkoxy, —OPO3H2, —O—C1-7alkanoyl or benzyloxy; and salts thereof in the manufacture of a medicament for use in the production of a vascular damaging effect in warm-blooded animals such as humans. The present invention further relates to compounds of the formula (I), pharmaceutical compositions containing them, processes for their preparation and to a method of treatment using the compounds to produce a vascular damaging effect in a warm-blooded animal such as a human. The compounds of formula (I) and the pharmaceutically acceptable salts thereof may be useful in the treatment of a number of disease states including cancer and rheumatoid arthritis.
EP2658549A1 Methods for reducing the incidence of oxidative stress using human milk oligosaccharides, vitamin c and anti-inflammatory agents Disclosed are methods of reducing the incidence of oxidative stress in infants, toddlers, and children using nutritional compositions including human milk oligosaccharides. The nutritional compositions including the human milk oligosaccharides are effective at reducing inflammation and the incidence of inflammatory diseases.
US20100184798 Methods to Predict Cholesterol Elevations during Immunosuppressant Therapy This invention provides methods to predict the degree of elevation of serum cholesterol levels in patients treated with immunosuppressive medication. This invention also provides treatment strategies based on these predictions and kits to carry out these methods.
US20100152201 Oligomer-Antihistamine Conjugates The invention provides antihistamine drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the antihistamine drug not attached to the water-soluble oligomer.
US6969708 Process for the preparation of a high purity composition comprising (7α, 17α)- 17-hydroxy- 7-methyl- 19-nor-17-pregn-5(10)-en-20-yn-3-one The invention pertains to a process for the preparation of a high purity composition of (7α, 17α)-17-hydroxy-7-methyl-19-nor-17-pregn-5(10)-en-20-yn-3-one. The process provides for a composition with less than 0.5% of (7α, 17α)-17-hydroxy-7-methyl-19-nor-17-pregn-4-en-20-yn-3-one. This composition can be used as a source for the preparation of stable pharmaceutical dosage units.
CN103058865A Crystal form and medicine composition of carboxylic acid derivative The invention relates to a crystal form and a medicine composition of a carboxylic acid derivative, and in particular to the following compound: the compound uses Cu-Kalpha radiation, and at least has a diffraction peak at about 5.18 degrees in a powder X-ray diffraction pattern which is expressed by using a 2theta angle. The compound provided by the invention can be used for treating or preventing retrogressive arthropathy, osteoarthritis and relevant diseases (the formula referring to the specification).
CN102160852A Ibuprofen injection and preparation method thereof The invention relates to an ibuprofen injection and a preparation method thereof. The ibuprofen injection is characterized in that the concentration of ibuprofen in the injection is 100mg/ml, arginine is used as a cosolvent, and the molar ratio of the arginine to the ibuprofen is greater than or equal to 1:1. The invention also provides a method for preparing the injection. The prepared injection which has good dissolvability is added into a 0.9% sodium chloride injection or a 5% glucose injection, the concentration of the ibuprofen is 4mg/ml or less than 4mg/ml, and the solution is clear and is stabilized for a long time. The ibuprofen injection is suitable for intravenous drip for patients for whom the oral administration is not suitable.
WO2014028025A1 Compositions and methods for treating myotonic dystrophy type 1 Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula (I) wherein X is selected from the group consisting of O, N, C, or S, Y is a homo- or heteroatomic 5-membered ring comprising one or more atoms selected from the group consisting of N, O, S, and C, Z is an optionally substituted aryl group or optionally substituted heteroaryl, including but not limited to halogenated benzenes, pyridines, substituted benzene, substituted pyridine, R2 = hydroxy, acyl, alkoxyl, esters, ethers, cyclic ethers, and lactones, R3 = H, alkyl, an optionally substituted alkyl, aliphatic ether, ester, cyclic unsaturated and aromatic ring groups, and R1, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, and alkoxyl or a pharmaceutically or cosmetically acceptable salt, solvate, or hydrate thereof.
CN101953847B Application of zinc hydroxide in preparation of anti-cancer drugs The invention provides application of a zinc hydroxide compound in preparation of anti-cancer drugs, in particular in the way of treating liver cancers. Through a zoology test, the zinc hydroxide has obvious anti-cancer effect on the liver cancer cells of mice and low toxic and side effects.
CN103127032A Tulobuterol patch The invention relates to a transdermal absorption preparation with anti-asthmatic drug tulobuterol and salt as active ingredients, in particular to a tulobuterol patch. The transdermal absorption preparation is capable of controlling release of the tulobuterol continuously and has long-term storage stability at the same time, and tulobuterol particles can not be formed on a drug layer.
CN103070921A Medicine for curing accumulated dampness-heat type cancerous fever The invention relates to a medicine for curing accumulated dampness-heat type cancerous fever. The medicine is prepared from the following raw materials in part by weight: 0.5 to 2.5 parts of radix scutellariae saponins, 0.18 to 0.75 part of berberine, 0.07 to 0.3 part of matrine, 6 to 24 parts of radix scutellariae, 6 to 24 parts of kuh-seng, 6 to 12 parts of radix tetrastigme, 3 to 9 parts of talc, 6 to 24 parts of bamboo leaf, 6 to 12 parts of poria cocos and 6 to 9 parts of lalang grass rhizome. The medicine has an obvious curative effect and no side effect when being used for curing excessive accumulated dampness-heat type cancerous fever.
WO2013057675A1 Alkenylglucosinolate detoxifying composition The present invention relates to an alkenylglucosinolate composition which under stomach conditions generates the corresponding epithionitrile derivative, which has detoxifying properties. It also relates to a food composition containing it, to the use of said composition as detoxifying agent and to a process for its preparation.
WO2012004677A1 Solid state forms of etoricoxib salts Provided herein are novel solid state forms of etoricoxib salts, process for their preparation, pharmaceutical compositions, and method of treating thereof. The etoricoxib salts include an oxalate salt, a succinate salt, a fumarate salt, a besylate salt, a hydrobromide salt, a glutamate salt, a sulfamate salt, a benzoate salt, a cinnamate salt, a salicylate salt, or a tosylate salt. The solid state forms of etoricoxib salts disclosed herein are useful for preparing etoricoxib free base with high purity.
EP2522665A1 Crystalline sodium salt of an HIV integrase inhibitor The present invention refers to a crystalline sodium salt of a compound of formula I (INN: Raltegravir) or a hydrate/solvate thereof as well as a process for obtaining the same.
US7854934 For treatment of cancer, preferably for prevention of recurrence of cancer, and for inducing antibodies in subject by administering glycopeptides The present invention provides novel glycosides and glycoconjugates, glycoamino acids, and methods for the synthesis thereof. In another aspect, the present invention provides novel clustered glycopeptides and methods for the synthesis thereof. In still another aspect, the present invention provides methods for the treatment of cancer, preferably for the prevention of recurrence of cancer, and methods for inducing antibodies in a subject, comprising administering to a subject in need, an effective amount of any of the inventive glycopeptides as disclosed herein, either in conjugated form or unconjugated and in combination with a suitable immunogenic carrier.
US20110130361 Silicon derivatives as histone deacetylase inhibitors The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the Silicon derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the Silicon derivatives in vivo.
CN1660112A Soft capsule of levogyrate ofloxacin and preparation method A 1-ofloxacin softgel withhigher curative effect and its preparing process are disclosed.
WO2013122855A1 Methods of increasing lymphatic transport Provided herein are methods of treating a lymphatic transport dysfunction or condition in a subject. Also provided are methods of preventing or reducing a flare in a subject with a lymphatic transport dysfunction or condition. Further provided are methods of monitoring lymphatic transport in a subject and methods of selecting a treatment protocol for a subject with a lymphatic transport dysfunction or condition. Further provided are methods of detecting a flare in a subject with a lymphatic transport dysfunction or condition.
CN102499938A Agonist and application of Toll-like receptors 7 and 8 The invention relates to an agonist and application of Toll-like receptors 7 and 8, wherein the agonist contains a nucleotide sequence segment with 17basic group characteristics, and has the basic structure of GUCUGAGUGUGUUCUUG. The agonist can combine specificity with TLR7/8, so the immune cells of an organism are promoted to efficiently release tumor necrosis factor (TNF)-a, interleukin (IL)-12, IL-6 and other cell factors, the immune function is up-regulated, and the agonist can be used for antiviral antineoplastic adjuvant therapy.
CN102861044A Novel application of himalayan teasel root chemical compositions The invention relates to novel application of himalayan teasel root chemical compositions and particularly relates to the application of himalayan teasel root chemical compositions for preparing medicines for preventing and/or curing bone diseases. The himalayan teasel root chemical compositions are one or more of cauloside A, 3-O-alpha-L-pyran arabinose- oleanolic acid-28-O-beta-D-pyran glucose-(1-6)-beta-D-pyran glucoside, loganin, secologanin and triplostosie A. The chemical components have exciting biological effects.
EP2336105A1 Nitrogen-containing heterocyclic compound and use of same The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and - - - is a single bond or double bond, or a salt thereof; and the like. The compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, digestive tract diseases, central neurological disease and the like.
WO2008049000A3 Combination therapy for pulmonary arterial hypertension Methods for treatment of pulmonary hypertension include administration of a first amount of treprostinil and administration of a second amount of a Rho kinase inhibitor such that the first amount and the second amount form together an amount effective for pulmonary hypertension treatment. Kits for treatment pulmonary hypertension are also disclosed.
WO2010006135A3 2-methylene-(17z)-17(20)-dehydro-19,21-dinor-vitamin d analogs This invention discloses 2-methylene-(17Z)-17(20)-dehydro-19,21 -dinor-vitamin D analogs, and specifically 2-methylene-(17Z)-17(20)-dehydro-19,21-dinor-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has significant calcemic activity in vivo having about the same bone calcium mobilization activity and intestinal calcium transport activity as the native hormone 1α,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
WO2006115134A1 Novel benzofuran derivative, pharmaceutical composition comprising the same, and use of the derivative or composition A compound represented by the general formula (I) or a prodrug or pharmacologically acceptable salt thereof. The compound (I) has an excellent adenosine A2A receptor antagonistic effect, and therefore is useful as a therapeutic or prophylactic agent for a disease associated with an adenosine A2A receptor, particularly movement disorder, depression, anxiety, cognitive disorder, ischemic cerebral disorder, restless legs syndrome or the like. (I) wherein R1 represents a hydrogen atom or a lower alkyl group; R2 represents -NR10R11 or -OR12; and R3, R4, R5 and R6 independently represent a hydrogen atom, a halogen, a lower alkyl group, a halo(lower) alkyl group, a lower alkoxy group, a hydroxyl group or the like.
US7112339 Compositions for controlled release of a biologically active agent, and the preparation thereof A composition for controlled release of a biologically active agent from a carrier. The biologically active agent is heparin or a related biologically active acidic polysaccharide and the carrier is a sol-gel derived silica xerogel. The xerogel is derived from a tetraalkoxysilane such as tetrethoxysilane (TEOS) and part of the tetraalkoxysilane is replaced by an organomodified alkoxysilane, preferably an akylsubsitituted alkoxysilane. The invention also includes a method for the preparation of this composition.
EP1303503B1 Aniline derivatives The present invention relates to compounds of formula (I) and pharmaceutically acceptable salt and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemmia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
WO2009089284A2 Substituted 2-aminotetralin derivatives as selective alpha 2b agonist Substituted 2-aminotetralin derivatives as selective alpha 2B agonists includes a compound represented by Formula (I): wherein R1 = H, methyl, ethyl, propyl, or cyclobutyl; R2 = methyl or H; R3 = pyridinyl X= C or O. The compounds of Formula 1 can be incorporated in a pharmaceutical compositions and can be used in methods of treating an alpha 2B receptor mediated diseases or conditions.
WO2007018660A3 Gabaergic imidazobenzodiazepine derivatives to treat memory deficits The present invention provides imidazobenzodiazepine derivatives and methods for the prevention and/or treatment of memory deficit related conditions and/or enhancement of cognizance. In a preferred embodiment, the invention includes compounds, salts and prodrugs thereof for the prevention and/or treatment of these conditions.
US20050070555 Aroyl pyridinones The present invention relates to pyridinones, processes for their preparation and their use in medicaments, especially for the treatment of COPD.
CN103028003A Preparation method of pharmaceutical tablet The invention relates to a preparation method of a pharmaceutical tablet. The preparation method of the pharmaceutical tablet disclosed by the invention comprises the following steps of taking prescription components such as fructus gardeniae, semen plantaginis, fringed pink, polygonum aviculare and talc according to a prescription proportion, extracting main active ingredients of the prescription components by methods of ethanol extraction, water boiling and the like, and adding a proper quantity of auxiliary materials for the formation of the tablet. The preparation method of the pharmaceutical tablet provided by the invention is simple; the extraction rate of the active pharmaceutical ingredients of the prescription components is high; the common production equipment can satisfy demand on the production of the pharmaceutical tablet; no specific equipment requirements are given; the production cost is lowered; and therefore, the patient burden is decreased.
WO2013187466A1 Branched chain alkyl heteroaromatic ring derivative A branched chain alkyl heteroaromatic ring derivative represented by formula (Ia) or a pharmaceutically acceptable salt thereof is useful for treatment or prophylaxis of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, cephalalgia, hemicrania, pain, digestive diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases and hypertension, on the basis of an orexin (OX) receptor antagonist activity.
WO2008058287A1 COMBINATION OF ERα+ LIGANDS AND HISTONE DEACETYLASE INHIBITORS FOR THE TREATMENT OF CANCER The present embodiments relate to compositions and methods of treatment of cancer. More particularly, the present embodiments relate to the combination of an ERα+ ligand with an HDACi for the treatment of cancer, methods of treating cancer and pharmaceutical compositions for treating cancer.
US20120015972 Indolizine derivative and use thereof for medical purposes The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R1 represents halogen, a hydroxy group or the like; R2 represents halogen, a hydroxy group, alkyl, alkoxy, alkyl substituted by fluorine, alkoxy substituted by fluorine or the like; m represents a number from 0 to 2; n represents a number from 0 to 3; and R3 represents hydrogen, fluorine or the like.
CN102000060B Application of E ring iodine substituted silybin to preparing glycosidase inhibitors The invention relates to application of E ring iodine substituted silybin to preparing glycosidase inhibitors and in particular discloses application of E ring iodine substituted silybin ester-type flavonolignans or pharmaceutical salt thereof to preparing drugs for inhibiting alpha-glycosidase and preventing and treating type II diabetes. The flavonolignans has extremely obvious activity for inhibiting alpha-glycosidase and the intensity of activity of the 40mcg/ml flavonolignans for inhibiting alpha-glycosidase reaches 64.1%. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 35 times that of the positive control drug acarbose. The pharmacodynamics result shows that the flavonolignans or pharmaceutical salt thereof can be expected to be applied to preparing glycosidase inhibitors, especially the drugs for preventing and treating type II diabetes.
WO2008033764A2 Quinazolinone and isoquinolinone acetamide derivatives The present invention relates to a quinazolinone or isoquinolinone derivative of formula I, wherein R1 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, C2-6alkenyl, C2-6alkynyl, said C1-6alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, C1-6alkyloxy, cyano or one or more halogens; R2 is C6-10aryl optionally substituted with one to three substituents selected from halogen, hydroxy, cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy and C3-6cycloalkyloxy, said C1-6alkyl, C3-6 cycloalkyl, C1-6 alkyloxy and C3-6Cycloalkyloxy being optionally substituted with one or more halogens; or R2 is a 5-10 membered heteroaryl ring system comprising a heteroatom selected from N, O and S and optionally substituted with a substituent selected from methyl, C1-6alkyloxy and halogen; or R2 is C4-7cycloalkyl; R3 is an optional substituent selected from C1-6alkyl, C1-6alkyloxy and halogen, said C1-6alkyl and C1-6alkyloxy being optionally substituted with one or more halogens; R4 is a group located at the 6- or 7- position of the quinazolinone or isoquinolinone ring having the formula Il, wherein R5 together with one of R6 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or R5 together with one of R7 and R8 forms a 6-8 membered heterocyclic ring optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; Each R6 is independently H, halogen or C1-4alkyl optionally substituted with halogen or SO2CH3 or one of R6 together with R5 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; R7 and R8 are independently H, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylc1-3alkyl, cyanoC1-3alkyl, C6-10aryl, C6-10arylC1-3alkyl, C1-3alkyloxyC1-3alkyl or C1-6acyl said C1-6alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, 1 or more halogens or diC1-2alkylamino; or R7 and R8 together with the nitrogen to which they are bonded form a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR10, said heterocyclic ring being optionally substituted with one or two substituents selected from C1-6alkyl, halogen, hydroxy, C1-6alkyloxy, cyano and COOR11; or one of R7 and R8 is Y, CH2Y or CH2CH2Y, wherein Y is a 4-6 membered saturated heterocyclic ring comprising a heterocyclic moiety selected from O, SO2 and NR10, said ring being optionally substituted with 1 -2 substituents selected from methyl or halogen; or one of R7 or R8 together with R5 forms a 6-8 membered heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or one of R7 and R8 together with R12 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroato
WO2009100723A3 Crystalline forms of an antibiotic substance Crystalline forms of 24-bromofusidic acid, their preparation, pharmaceutical compositions containing them, and the use of said crystalline 24-bromofusidic acid forms as medicaments in the treatment of infectious diseases.
DE102010052939A1 Ointment-shaped agent, useful e.g. as pain relieving ointment, comprises a carrier substance and many substances comprising heparin, hydroxyethyl salicylate, diclofenac, and essential oil and/or at least a part of the essential oil Ointment-shaped agent comprises a carrier substance and many substances comprising heparin, hydroxyethyl salicylate, diclofenac, and at least an essential oil and/or at least a part of the essential oil. - ACTIVITY : Analgesic. - MECHANISM OF ACTION : None given.
CN101824068A Cyclic-ahltin type triterpenoid saponin compound and preparation method and application thereof The invention belongs to the technical field of medicines and provides a cyclic-ahltin type triterpenoid saponin compound and a preparation method and application thereof. The cyclic-ahltin type triterpenoid saponin compound is prepared by the steps of: obtaining an extracting solution or extract liquor by using a flash extraction technology or a solvent extraction method; processing the extracting solution or the extract liquor by using a non-polar resin column to obtain crude saponin; quickly processing the crude saponin by using a silica gel flash column chromatography, and then carrying out solvent gradient elution, and further separating and purifying by using a medium-low pressure column chromatography or open ODS (Oxide Dispersion Strengthened) column chromatography and an HPLC (High Performance Liquid Chromatography) technology. An LC-MS technology is used for detecting the components of the cyclic-ahltin type triterpenoid saponin compound in the preparation process. The prepared cyclic-ahltin type triterpenoid saponin compound has better anti-tumor activity.
WO2014031026A1 Method for restoring male sex drive (libido) using a food supplement for restoring male sex drive (libido) The method for restoring male sex drive (libido) using a food supplement for restoring male sex drive (libido) relates to medicine, and more specifically to the pharmaceutical industry producing food supplements for restoring male sex drive (libido) and male sexual function which are based on natural ingredients. The method involves the use of nitric oxide (NO) in terms of L-arginine, pollen or beebread in terms of rutin, drone brood in terms of decenoic acids, a substance containing zinc in terms of zinc, a substance containing vitamin B6 in terms of vitamin B6, horny goat weed in terms of icariin, true or false ginseng root in terms of saponins, and leuzea or crowned saw-wort in terms of ecdysteroids, in various combinations.
EP1604663A1 Zolpidem Hemitartrate Form H Solvate The present invention provides novel forms of zolpidem hemitartrate.
US20090069410 Deuterium-enriched paclitaxel The present application describes deuterium-enriched paclitaxel, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20080214491 Methods of Inhibiting the Interaction Between S100 and the Receptor for Advanced Glycation End-Products A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. In some embodiments, the S100 protein is S100P. In some embodiments, the S100 protein is S100P. In addition, the present invention provides a method of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. Additional methods are also provided.
US7192980 Such as 6-[14-[(aminocarbonyl)oxy]-2,6,12-trihydroxy-5,7,9,11,13,15-hexamethyl-3,8,16,18-nonadecatetraenyl]tetrahydro-(6R)-2H-pyran-2-one; high selectivity; colon cancer The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.
CN1981770A Olea acid dropping balls and their production A dripping pill of caryophyllin is disclosed. Its preparing process includes such steps as mixing PEG 6000, PEG 4000 and tween-80 by grinding, heating for fusing, adding caryophyllin, stirring, heating for fusing, dripping in dimethyl silicon oil at 5-15 deg.C, removing dimethyl silicon oil from its surface by dried filter paper, and drying.
CA2380924C Compositions for treating viral infections, and methods therefor Methods and combinations of an agent that promotes DNA synthesis in a virally-targeted cell and a nucleoside analogue having antiviral activity are provided for treating a viral infection in a subject in need thereof. Such compositions are particularly effective where the subject has resistance to a nucleoside analogue, where the subject has resting cellular reservoirs of such a virus, or to induce a post-treatment period of replication incompetence of such a virus.
WO2011134538A1 Diyne compositions A novel class of diyne compounds and diyne salts provided herein are effective and potent Ole1 protein inhibitors, useful for treating fungal pathogens. Compounds, fungicides and methods are provided as novel, potent and broad spectrum antifungal agents for treatment against a wide variety of fungal pathogens in humans and animals, and in the agricultural setting.
US20100151001 Ethynylated heterodinucleoside phosphate analogs, method for the production thereof, and use thereof The invention relates to novel ethynylated heterodinucleoside phosphate analogs, the production thereof, substances containing at least one of said compounds, and the use thereof for the treatment of cancer and infectious diseases.
CN103060271A Application of naringin in promoting proliferation and differentiation of neural stem cell The invention belongs to the field of regenerative medicine and pharmacology, relates to an application of a double hydrogen flavonoid small molecule compound, and particularly relates to a new application of naringin in promoting proliferation and differentiation of a neural stem cell. The invention is characterized by relating to an application of the naringin in medicament for neural stem cell transplantation in the treatment of neurodegenerative diseases, an application of the naringin in repairing damaged nerve tissues and preparation a function-reconstructable nerve nutriment and cell differentiation agent, and an application of the naringin in constructing an efficient medicament screening model and applying the efficient medicament screening model to preliminary screening and evaluation of the medicament efficacy. The invention confirms the new pharmacological activity of the naringin, establishes an application foundation in stem cell transplantation (SCT), and provides new thoughts for developing new medicaments with independent intellectual property rights.
CN103601697A 4-tertiary butyl-5-(2-nitroethyl)-2-acylamino thiazole and preparation method and application thereof The invention relates to 4-tertiary butyl-5-(2-nitroethyl)-2-acylamino thiazole or salts thereof shown in the chemical formula I or II; in the formula, Y1 is H, methyl, ethyl, fluorine, chlorine or bromine; Y2 and Y4 are H, methyl or ethyl; Y3 is fluorine, chlorine or bromine; and R is C1-C2 alkyl, C3-C17 straight chain alkyl or branched alkyl, C1-C2 chlorinated alkyl, C3-C5 chlorinated straight chain alkyl or chlorinated branched alkyl. 4-tertiary butyl-5-(2-nitroethyl)-2-aminothiazole is acylated to prepare the 4-tertiary butyl-5-(2-nitroethyl)-2-acylamino thiazole; and the invention also provides an application of the 4-tertiary butyl-5-(2-nitroethyl)-2-acylamino thiazole or salts thereof in preparation of anticancer drugs.
WO2009155139A9 Use of isoindoles for the treatment of neurobehavioral disorders The present invention generally relates to the use of drugs for the treatment of neurobehavioural disorders or symptoms of a neurobehavioural disorder associated with dysfunction of the trimonoamine modulating system (TMMS). More specifically, the invention describes method for the treatment of a neurobehavioural disorder and/or treatment or prevention of symptoms of a neurobehavioural disorder by administering suitable Isoindole derivatives, such as Mazindol, alone or in combination with other agents so as to provide relatively equal inhibitory effect on serotonin, dopamine and norepinephrine.
US20110182891 Pharmaceutical dosage form comprising polymeric carrier composition A pharmaceutical dosage form comprises a solid dispersion product of at least one active ingredient dispersed in a polymeric binder composition, the polymeric carrier composition comprising a) a vinylpyrrolidone homopolymer, wherein at least 95% by weight of the vinylpyrrolidone homopolymer has a molecular weight distribution within the range of from 1000 to 13 000; and b) a vinylpyrrolidone copolymer having a weight-average molecular weight of from 5000 to 1 500 000. The dosage form is preferably prepared by a melt extrusion process. The polymeric carrier composition exhibits a high drug dissolution power and allows a reduction of the viscosity of the melt without deteriorating the mechanical properties and storage stability of the dosage form.
US20070265228 decreases expression of a Type I collage gene in a tissue to induce a reduction in accumulation of collagen and thereby improves tissue fibrosis The present invention relates to a cinnamoyl compound represented by the formula (I):
US7820687 inflammatory diseases such as asthma, Alzheimer's disease, atherosclerosis, diabetes, autoimmune diseases, tumor metastasis and myocardial ischemia; improved bioavailability; 2-(2-(diethylamino)-5-(N-isopropylmethylsulfonamido)pyrimidin-4-ylamino)-3-(4-(pyrrolidine-1-carbonyloxy)phenyl)propanoic acid Disclosed are compounds, which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
CN103006705A Haemorrhoids paste and preparation method thereof The invention relates to the field of medicine, and in particular relates to a haemorrhoids paste and a preparation method thereof. The haemorrhoids paste can be used for shortening the cure course and comprises the following ingredients in parts by weight: 100-200 parts of badger fat, 1.5-4 parts of borneol, 1-3 parts of water, 0.1-0.4 parts of ammonium glycyrrhetate, 0.8-1.5 parts of vitamin B1, 0.8-1.5 parts of vitamin B2, 0.05-0.15 parts of vitamin B6 and 0.05-0.25 parts of anisodamine; the badger fat is molten within 40-60 DEG C; the molten badger fat is filtered; the borneol is added into the filtered badger fat so as to form a first mixture after the borneol is completely molten; ammonium glycyrrhetate, vitamin B1, vitamin B2, vitamin B6, and anisodamine are added into the 1-3 parts of water to be mixed and prepared into a first mixture solution; and the first mixture solution and the first mixture are mixed and uniformly stirred so as to form the haemorrhoids paste provided by the invention.
CN101269011A Tiopronin injection and preparation method thereof The invention belongs to the technical field of medicament and provides a tiopronin injection and a preparation method thereof. The tiopronin injection includes the constituents with the shares by weight: 1 share of sodium calcium edetate; 50 to 200 shares of tiopronin. The preparation method of the tiopronin injection provided by the invention comprises the following steps that: a. the sodium calcium edetate and the tiopronin which have the proportioning by weight of 1:50 to 200 are added with water for injection to be stirred and dissolved under the protection of nitrogen; b. the solution is added with needle activated carbon having the liquid rate with the weight percentage composition of 0.04 to 0.1 percent as well as is added with nitrogen to be stirred for 10 to 30 min and then is filtered by a microporous filtering film, the pH value is measured and adjusted to be 1.0 to 3.0; the mixture is replenished with water for injection to the quantity of medical prescription and then is filled with nitrogen for encapsulation and filtered to made into injecta preparation. The tiopronin injection and the preparation method thereof have the advantages of (1) good stability, convenient storage and long period of validity; (2) qualified related material and no potential possibility causing other side effects; (3) simple technique and easy manufacturing production.
CA2151443C Cycloheptimidazole derivatives, method of manufacturing the same and therapeutic agents containing these compounds Cycloheptimidazole derivatives of following general formula, (See formula I) (Wherein R1 is represents a lower alkyl, R2 represents tetrazole) method of manufacturing the same and therapeutic agents containing these compounds.New cycloheptimidazole derivatives of the present invention have angiotensin II receptor antagonistic activities and are therefore useful as treatment agent for hypertension or congestive heart failure or intraocular pressure lowering agent are proposed.
US20070298125 Medical Solution, A Method For Producing Said Medical Solution And Use Thereof The present invention relates to a medical solution, a method for producing said medical solution, a multi-compartment bag containing the medical solution as well as use of said medical solution. According to the invention the medical solution comprises a first single solution comprising bicarbonate and carbonate in such proportions that the partial pressure of carbon dioxide, CO2, in the first single solution is of the same order of magnitude as the partial pressure of carbon dioxide, CO2, of the atmosphere. The medical solution further comprises a second single solution comprising an acid. Said first and second single solutions are, after terminal sterilization and up on use, to be mixed to form a final solution. Said second single solution has a pH of 1.0-1.5, and said final solution has a pH of 7.0-7.6.
WO2013015979A2 Compositions containing zinc salts and isothiocyanates for reduction of oral volatile sulfur compounds (vscs) Combinations of a zinc salt and an isothiocyanate are provided, and more particularly to a consumer acceptable oral composition containing such combination which is effective in the reduction of volatile sulfur compounds (VSCs).
US20130041020 Methods of Control and Prophylaxis of Inflammation and Mitigation of Inflammatory Conditions in Companion Animals The invention relates to methods of control and prophylaxis of inflammation and mitigation of inflammatory conditions, particularly arthritis and joint pain, in companion animals, e.g., dogs or cats, comprising administering a diet comprising lipoic acid.
CN101703503A Application of organic dicarboxylic acid salts in preparing medicaments for preventing and treating cataract The invention aims to provide application of organic dicarboxylic acid salts, namely new application in pharmacy, in particular application in preparing medicaments for preventing and treating cataract. New anti-cataract active components in No.1, No.2, No.3, No.4, No.6, NO.7, No.8 and No.9 compounds are discovered by screening rabbit and rat H2O2 induced cataract and rat xylose induced cataract models, and the medical application of the compounds in preparing the medicaments for resisting oxidative damage and sugar metabolism disorder induced cataract is discovered. The No.4 compound has strong and high effect of resisting phacoscotasmus, and has good medicinal prospect. The No.4 compound has obvious effects of improving rabbit lens water-soluble proteins (sol-pro) and total antioxidant capacity (T-AOC), and reducing malondialdehyde (MDA), so the effect of the No.4 compound of resisting H2O2 induced lens oxidative damage is related to the strong oxidation resistance of the No.4 compound.
CN1582960A Composite medicine for tooth diseases A composite medicine for treating gingivitis, toothache, etc is prepared from 4 Chinese-medicinal materials including cinnabar, borax, exicaated sodium sulfate, etc through proportional mixing and pulverizing.
US20100316718 Activated foam The present invention relates to an activated foam made of a natural or synthetic rubber or a synthetic resin, characterized in that the foam contains a zirconium compound and/or a germanium compound, and has a closed-cell structure, wherein the foam is used so as to directly or indirectly contact with a human body when a pharmaceutical agent is administered. The activated foam can be directly or indirectly contacted with a human body to facilitate blood circulation and promote the improvement of physical condition and the cure of diseases. It also has no adverse effect.
US20060105378 Tenascin-C nucleic acid ligands Methods are described for the identification and preparation of nucleic acid ligands to tenascin-C. Included in the invention are specific RNA ligands to tenascin-C identified by the SELEX method. Further included in the invention are methods for detecting the presence of a disease condition in a biological tissue in which tenascin-C is expressed.
CA2305762C Delayed total release gastrointestinal drug delivery system A gastrointestinal delivery system is provided. The system comprises a drug in combination with a swellable core material, the core being surrounded by a water-insoluble or relatively water-insoluble coating material in which particulate water-insoluble material is embedded. When the delivery device enters the gastrointestinal tract, the particulate matter takes up liquid, thus forming channels interconnecting the drug-containing core with the outside of the delivery device. Through these channels liquid enters the core which then swells to the point at which the coating is broken. When the integrity of the coating is destroyed, the core then disintegrates immediately releasing all or most of the drug at a specific site. By controlling parameters in the device, such as the core material, carrier material in the coating, and particulate matter, the location of release of the drug can be carefully controlled. Thus, the invention is also directed to a method of using the device for the treatment of disease by the release of drugs in the gastrointestinal tract in a location- and time-dependent manner.
WO2011011252A1 Methods of attenuating the loss of functional status Nutritional compositions and methods of using the nutritional compositions with exercise to attenuate the loss of functional status are provided. In a general embodiment, the present disclosure provides a nutritional composition including whey protein, and Vitamin D. The nutritional composition and exercise can be specifically used to attenuate the loss of functional status, especially in the elderly.
US7534793 (R)-2-{4-[(1H-Indol-2-ylmethyl)-amino]-piperidin-1-yl}-1-(6-methoxyquinolin-4-yl)-ethanol; effective against both gramnegative and grampositive bacteria Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man
WO2014080378A1 Phenothiazine derivatives and their use against tuberculosis Tricyclic derivatives of formula (1), wherein R1 may be an alkyl sulphonate or sulphonamide group, are useful as antimicrobial agents. The derivatives are optionally substituted wherein R2 is a hydrogen, a halogen, a substituted alkyl group, a thioether or an acetyl group; Y may be N, or C; X may be S, SO, SO2, N, O, CH2, C(O), CO2, NHCO, and ring B is a 6, 7 or an 8 membered cycloalkyl ring. The tricyclic derivatives, such as phenothiazine derivatives, may be used in treating tuberculosis, especially drug sensitive and resistant forms of tuberculosis. The derivatives of the invention may be used independently or in combination with known anti-tubercular drugs such as isoniazid, ethionamide and ethambutol, and the combination may be administered as a single dose, or as two independent dosages. The tricyclic derivatives may also be used for the manufacture of a medicament for treating tuberculosis.
WO2010053655A2 Therapeutic methods with withaferin a and analogs Compounds of Formulas 1 (withaferin A, also referred to as D004), 2 (viscosalactone B, also referred to as E002), and 3 (22R-5β-formyl-6β,27-dihydroxyl-l -oxo-4-norwith-24- enolide, also referred to as O010), as well as salts, prodrugs, analogs, and derivatives thereof are biologically active for modulating Hsp70, Hsp90, and/or HSFl. Also, these compounds can be included in pharmaceutical compositions for administration to a subject for modulating the expression or activity of Hsp70, Hsp90, and/or HSFl in order to produce a therapeutic effect.
CN103381169A Applications of Chukrasone A in anti-tubercle bacillus medicines The invention discloses applications of Chukrasone A in preparation of anti-tubercle bacillus medicines. At present, morbidity of tuberculosis is high, mycobacterium trberculosis multiple-resistant strains are found, and morbidity and mortality of tuberculosis are on the rise, so that application prospect of the remarkable inhibitory activity of Chukrasone A on tubercle bacillus is promising. The applications of Chukrasone A in preparation of anti-tubercle bacillus medicines are disclosed for the first time. Due to the fact that skeleton type belongs to completely novel skeleton type, and Chukrasone A has an unexpectedly high inhibitory activity on tubercle bacillus, probability of other compounds giving any revelation for Chukrasone A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in treating of tubercle bacillus infection.
EP1781284B1 Use of the combination comprising temozolomide and tnf-alpha for treating glioblastoma Disclosed are methods of synergistically inhibiting growth of a glioma cell comprising contacting the cell with temozolomide and TNFα, or with temozolomide, TNFα, and radiation. Also disclosed are methods of synergistically inhibiting growth of a glioma in a human cancer patient comprising administering temozolomide and TNFα, or with temozolomide, TNFα, and radiation. Pharmaceutical combinations and therapeutic combinations suitable for use in the methods of the invention are also disclosed.
CN1792363A Medicinal composition contg. IDV and valproic acid or salts thereof A composite medicine for treating AIDS and ARC and killing HIV is prepared from the Yindinawei (0.1-95 Wt%), propylphocenic acid or its salt (10.-95), and medicinal auxiliary (4-98.9).
CN1931178A Pirarubicin liposome and its prepn process The present invention relates to one kind of pirarubicin liposome and its preparation process. Pirarubicin possesses relatively high antitumor effect but certain toxic side effect, and the present invention aims at providing one kind of pirarubicin liposome with obvious curative effect, less toxic side effect and good targeting. The pirarubicin liposome consists of medicine component and supplementary material, the medicine component is pirarubicin or pirarubicin hydrochloride, and the supplementary material includes phospholipid and cholesterol. It may be in injection or freeze dried preparation. The pirarubicin liposome is used in treating different kinds of cancer, such as bladder carcinoma, leukemia, mammary cancer, liver cancer, gastric cancer, etc. and has relatively high curative effect.
WO2005025620A3 Combination therapy with inhibitors of inducible nitric oxide synthase and alkylating agents A combination therapy comprising administration of a carbamoylating chemotherapeutic agent in conjunction with administration of a selective iNOS inhibitor compound is disclosed. Optionally, resection and radiation therapy are provided with the therapeutic combination. A medicament comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound together with a pharmaceutically acceptable carrier is further disclosed. A kit comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound is further disclosed.
WO2008071245A1 Pharmaceutical preparation for the treatment of inflammatory diseases of the urogenital tract The invention relates to a pharmaceutical composition which is suitable in particular for the treatment of inflammatory diseases of the urogenital tract, preferably of cystitis. The composition according to the invention comprises, in combination and in each case in pharmaceutically effective amounts, hyaluronic acid and/or salts thereof, preferably with an average molar mass (molecular weight) of less than 200 kDa, and at least one further glycosaminoglycan different therefrom, preferably at least one chondroitin sulphate.
WO2008147228A1 Treatment or prevention of bone conditions Use of carboxyhc acids, or salts thereof, or ester or ether, amide, amine, ketone or aldehyde derivatives thereof, or free fatty acids, lipids, lipid compositions or dairy lipid fractions to treat or prevent conditions likely to benefit from a reduction in bone resorption or an increase in osteoblast proliferation.
WO2005103710A3 Diagnostics and therapeutics for diseases associated with corticotropin releasing hormone receptor 1 (crhr1) The invention provides a human CRHR1 which is associated with the hematological disorders, neurological disorders, developmental disorders, urological disorders and reproduction disorders. The invention also provides assays for the identification of compounds useful in the treatment or prevention of hematological disorders, neurological disorders, developmental disorders, urological disorders and reproduction disorders. The invention also features compounds which bind to and/or activate or inhibit the activity of CRHR1 as well as pharmaceutical compositions comprising such compounds.
US20090208939 Identification of Molecular Diagnostic Markers for Endometriosis in Blood Lymphocytes The invention comprises a method of identifying or predicting the predisposition to endometriosis in a female subject comprising determining the level of gene expression of at least one differentially-expressed gene or protein or peptide of peripheral blood leukocytes in a sample of peripheral blood leukocytes or peripheral blood in a subject to provide a first value, determining the level of gene expression of the at least one differentially-expressed gene or protein or peptide of said leukocytes in a control or reference standard to provide a second value, and comparing whether there is a difference between the first value and second value.
WO2012119941A1 Peptidyl nitrilcompounds as peptidase inhibitors The invention relates to compounds of Formula (II) and their use in theraphy as peptidase inhibitors.
CN101855209A Alkylsulfone derivative Disclosed is a compound which has an activity of inhibiting the production/secretion of beta-amylolid protein and is effective for the prevention/treatment of a disease associated with the production/abnormal secretion of beta-amylolid protein. Specifically disclosed is a compound represented by the general formula (I), a salt thereof, or a solvate of the compound or the salt. (I) wherein R1 represents a C1-C6 alkyl group which may have 1 to 6 halogen atoms as substituents, a C2-C6 alkenyl group which may have 1 to 6 halogen atoms as substituents, or a C3-C7 cycloalkyl group which may have 1 to 6 halogen atoms as substituents; R2 represents a 6-membered nitrogenated monocyclic aromatic heterocyclic group having 1 to 3 substituents, or a 9- or 10-membered nitrogenated bicyclic heterocyclic group having 1 to 4 substituents; Z1, Z2 and Z3 independently represent a hydrogen atom, a halogen atom or a cyano group; and n represents a number of 0, 1 or 2.
CN101919808A Topical fluorouracil vesicle gel and preparation method thereof The invention relates to a fluorouracil vesicle gel which is prepared by using fluorouracil, PlronicF68, Span and other surfactants, cholesterols and the like to prepare vesicle suspension in the self-assembly way, and further using carbomer and other excipients to prepare the vesicle gel, and the fluorouracil vesicle gel can be topically applied o the skin for treating various viral warts, keratosis, skin cancer, psoriasis, keloid, melanoma and other diseases. The prepared vesicle has complete shape and relatively uniform particle size distribution, and the encapsulation rate is 23.48%-51.14%. The vesicle gel has good uniformity and stable nature, and excised skin test results of rats and mice prove that the vesicle gel can significantly increase the retention of a drug in the skin and have the sustained release property, indicating that the fluorouracil vesicle gel has high utilization rate of the drug in the topical part of medication and significant sustained release effect of a drug storage library, and is conductive to reducing the systemic toxicity and side effects and improving the efficacy.
US20080207690 Benzisoxazole Derivatives This invention relates to compounds of the formula (I): wherein A, B, R1, R4, m, and n are each as described herein or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central 10 nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
CN101108872B Plants natural base extract and formulated product and use thereof A botanical alkaloid extractive is provided, which is characterized in that the extractive is extracted from the and / or fruits, or solanum nigrum or solanum xanthocarpum. The invention also discloses a medicine of any form receivable pharmaceutically and mixedly produced by the botanical alkaloid extractive and the drug carriers receivable pharmaceutically. The extractive of the invention has scientific and reasonable extracting steps and has little impurity content and high content of the active ingredient solamargine with minimum of 90.0 per cent and maximum of 99.9 per cent. Certified bythe test, the extractive preparation of the invention is safe and effective and controllable in quality.
CN103156809A Furosemide injection and preparation method thereof The invention discloses a furosemide injection and a preparation method thereof, and particularly provides the furosemide injection containing methionine, sodium chloride, polyethylene glycol 400 and sodium hydroxide and the preparation method thereof. The methionine serves as antioxygen, the sodium chloride serves as an isoosmotic adjusting agent, the polyethylene glycol 400 serves as stabilizer, and the sodium hydroxide solution at concentration of 10 per cent is used for adjusting the potential of hydrogen (PH) of the injection to 9.3-9.5. The injection prepared through the preparation method of can keep the content of effective elements being stable, visible foreign matters are qualified and related substances do not increase in placement, the external properties of the injection meet the specification, and safety and effect of medication to a patient are guaranteed.
WO2014150252A1 Methods of treatment associated with the granulocyte colony-stimulating factor receptor Some embodiments include methods for treating, preventing, reversing, halting, or slowing the progression of cancer, comprising administering to a subject in need thereof an effective amount of one or more chemotherapeutic agents, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition, wherein at least one of the chemotherapeutic agents is a cytotoxic granulocyte colony-stimulating factor receptor (GCFR) modulator. Methods are also disclosed for treating, preventing, reversing, halting, or slowing the progression of a hematopoietic disorder, comprising administered a therapeutically effective cytotoxic amount of a GCFR modulator to a subject in need thereof.
US20110183907 Factor viii, von willebrand factor or complexes thereof with prolonged in vivo half-life The present invention relates to modified nucleic acid sequences coding for coagulation factor VIII (FVIII) and for von Willebrand factor (VWF) as well as complexes thereof and their derivatives, recombinant expression vectors containing such nucleic acid sequences, host cells transformed with such recombinant expression vectors, recombinant polypeptides and derivatives coded for by said nucleic acid sequences which recombinant polypeptides and derivatives do have biological activities together with prolonged in vivo half-life and/or improved in vivo recovery compared to the unmodified wild-type protein. The invention also relates to corresponding FVIII sequences that result in improved expression yield. The present invention further relates to processes for the manufacture of such recombinant proteins and their derivatives. The invention also relates to a transfer vector for use in human gene therapy, which comprises such modified nucleic acid sequences.
US20120159657 Compositions and Methods for Inhibiting Expression of RRM2 Genes The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a RRM2 gene. The invention also relates to a pharmaceutical composition comprising the dsRNA or nucleic acid molecules or vectors encoding the same together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of a RRM2 gene using said pharmaceutical composition; and methods for inhibiting the expression of RRM2 in a cell.
WO2006077426A2 4- (2, 6-DICHLOROBENZOYLAMINO) -lH-PYRAZOLE-3 -CARBOXYLIC ACID PIPERIDIN- 4 -YLAMID ACID ADDITION SALTS AS KINASE INHIBITORS The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-lH- pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-lH- pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4- (2,6-dichloro-benzoylamino)-lH-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates.
EP2409984A1 Dimeric IAP Antagonists The present invention provides IAP antagonists that are peptidomimetic compounds that mimic the tertiary binding structure and activity of the N-terminal four amino acids of mature Smac to lAPs.
EP2634178A1 Quinazoline derivative and quinazoline complex protein kinase inhibitor for inhibiting multiplication of tumor cells and preparation method thereof Quinazoline derivatives represented by general formula (1) and quinazoline complexes as protein kinase inhibitors, and their preparation methods are provided. Wherein, in general formula (1), at least one of R and R' is a group containing an atom capable of coordinating with noble metals, m and n are either the same or different and are integers from 0 to 5. Said quinazoline complex as protein kinase inhibitor is formed by coordination compound containing noble metal and said quinazoline derivative ligand capable of coordinating with noble metal in the coordination compound. Used as tyrosine protein kinase inhibitors, Quinazoline derivatives and quinazoline complexes as protein kinase inhibitors provided by the present invention have exhibited good inhibitory effect on proliferation of various tumor cells including human breast cancer cells line (drug-resistant) MCF-7/A, human breast cancer cell line (sensitive) MCF-7/S, prostate cancer cell PC-3, keratinocytes Colo-16, human non-small cell lung cancer cell line A549, etc.
WO2009040819A2 DOWN-REGULATION OF MORTALIN BY siRNA Use of a siRNA molecule selected from the group consisting of SEQ ID NO: 173 to 344 for treating a disease associated with a pathological cell population in a subject in need thereof is disclosed.Pharmaceutical compositions and articles of manufacture comprising the siRNAs are also disclosed.
CN101966175A Application of dehydroabietic silybin in preparing glycosidase inhibitors The invention relates to the application of dehydroabietic silybin in preparing glycosidase inhibitors, in particular to an application of dehydroabietic silybin flavanolignan or pharmaceutically acceptable salts thereof in preparing medicaments for inhibiting alpha-glycosidases and preventing type-II diabetes (namely, non-insulin-dependent diabetes). The flavanolignan has a significant activity for inhibiting the alpha-glycosidase; through measuring the half inhibition concentration of the flavanolignan, the measurement results show that: the strength of the flavanolignan for inhibiting the alpha-glycosidase is over 36 times of that of acarbose (a positive control medicament), and the pharmacodynamic result shows that the flavanolignan or the pharmaceutically acceptable salts thereof can be predictably used for preparing the glycosidase inhibitors, especially the medicaments for preventing and treating the type-II diabetes (namely, the non-insulin-dependent diabetes).
CN102793718A Pharmaceutical composition including aspirin salt and aluminium magnesium salt The invention relates to a novel pharmaceutical composition consisting of 1-1000 mg of a pharmaceutically acceptable salt or ester of aspirin, 1-500 mg of heavy magnesium carbonate, 1-500 mg of dihydroxyaluminium aminoacetate and at least one pharmaceutically acceptable vector, wherein the pharmaceutically acceptable salt or ester of is arginine aspirin or lysine aspirin. The pharmaceutical composition can be used for treating unstable angina pectoris, acute myocardial infraction, local ischemic cerebrovascular disorders, headache, toothache, dysmenorrheal, arthralgia, neuralgia or cold and fever. With a combination of the above three components, adverse effects of aspirin can be effectively reduced; and simultaneously medical compliance of patients is improved.
CN1346281B Use for preparing medicine used for the planned stimulation to controlled ovary A method of therapeutic management of infertility by programming of controlled ovarian stimulation (COS) and assisted reproductive procedures (ART) the improvement consisting of a) supression of premature ovulation with an LHRH-antagonist in controlled ovarian stimulation (COS) and assisted reproductive techniques (ART) with multiple follicle and oocyte development; b) programming the start of controlled ovarian stimulation (COS) by the administration of progestogen only - or alternatively combined oral contraceptive preparations; c) exogenous stimulation of the ovarian follicle growth; d) ovulation induction with HCG, native LHRH, LHRH-agonists or recombinant LH; e) application of assisted reproduction techniques, especially of IVF, ICSI, GIFT, ZIFT or by intrauterine insemination by sperm injection.
US20080132533 Solid Dispersion Comprising Tacrolimus and Entericcoated Macromolecule This invention relates to a solid dispersion formulation comprising tacrolimus and enteric polymer. The solid dispersion formulation may contribute to better stability of tacrolimus preparation under high temperature and humidity condition through reduced recrystallization rate of tacrolimus. In addition, the solid dispersion formulation releases tacrolimus immediately in aqueous media and elevated solubility level maintains for certain period of time and that way the formulation may also enhance the bioavailability and oral absorption rate of tacrolimus.
US20110236475 Granular pharmaceutical compositions Pharmaceutical compositions comprising a plurality of formulated particles containing at least one active ingredient and at least one pharmaceutically acceptable excipient, granulated with a granulating composition containing at least one pharmaceutical excipient.
CN101040868A Preparation for regulating release of lithium carbonate, and method for preparing the same Modified release formulation of lithium carbonate in microgranules or similar comprising, for around 300 Kg of Lithium Carbonate, at least: Overall Povidone in quantity between 8.0 Kg and 40.0 Kg; Ethylcellulose in quantity between Kg 0.9 and Kg 3.6.
CN102949377A Acetazolamide sustained-release capsule and preparation method thereof The invention discloses an acetazolamide sustained-release capsule and a preparation method thereof. The acetazolamide sustained-release capsule is mainly composed of the following raw materials in accordance with parts by weight: 65 to 85 parts of acetazolamide, 15 to 35 parts of microcrystalline cellulose and 0.1 to 0.5 part of sodium dodecyl sulfate, and the acetazolamide sustained-release capsule further contains pharmaceutically acceptable pharmaceutic adjuvants. The preparation method comprises the following steps that the required raw materials and the adjuvants are smashed and uniformly mixed, and then the raw materials and adjuvants are prepared into soft materials after being uniformly mixed; a low-temperature refrigerator is turned on, the soft materials are put into an extrusion rolling machine to be extruded and rolled, and then drug containing micro pills with uniform particle sizes are formed; after the drug containing micro pills are dried, acetazolamide sustained-release micro pills are obtained; and the acetazolamide sustained-release micro pills are encapsulated to obtain the acetazolamide sustained-release capsule. The acetazolamide sustained-release capsule prepared by using the preparation method has little side effect and is convenient for patients to treat for a long time, and the drug compliance is improved. When the acetazolamide sustained-release capsule is taken once a day, the concentration of effective drugs in vivo can be guaranteed for 24 hours, and the toxic and side effects caused by a higher peak value of the blood drug concentration due to normal preparations can be reduced.
DE102010026883A1 Transdermal system useful e.g. for indication of breast cancer with progesterone-receptor positive status, comprises e.g. aromatase inhibitor, active substance puller protection layer, active substance reservoir Transdermal system comprises: at least one aromatase inhibitor as an active substance, preferably at least one active substance from non-steroidal and steroidal aromatase inhibitors and group formed from their derivatives; an active substance puller protection layer; an active substance reservoir; an optionally active substance permeable membrane; and a carrier for an active substance reservoir or an optional membrane.
WO2011009899A3 Phenalenones as antitumoral agents Compounds of general formula (Ia) or (Ib) or (Ic) or (Id), wherein the R groups are each independently selected from the group consisting of hydrogen, acyl, alkyl, alkenyl, alkynyl, aryl, -CONH2, alkali metal, and sugar, and their use for the treatment of cancers.
WO2009063897A1 Prophylactic or ameliorating agent for psoriasis in the skin The object is to provide a safe and highly effective prophylactic or ameliorating agent for psoriasis in the skin. Thus, provided is a prophylactic or ameliorating agent for psoriasis in the skin, which comprises a compound represented by the general formula (I) or a salt thereof as an active ingredient. (I) wherein R1, R2 and R3 independently represent a lower alkyl, a lower alkenyl, a lower alkynyl, an aralkyl, an araryl, a phenyl or a hydrogen atom.
US20080146538 exo-3-Bromo-N-((2S)-2-(4-fluorophenyl)-4-(3-(3-hydroxy-8-azabicyclo[3.2.1]oct-8-yl)azetidin-1-yl}butyl)-N-methyl-5-(trifluoromethyl)benzamide;neurokinin NK/tachykinin receptor antagonist; neurodegenerative diseases, antidepressant; gastrointestinal disorder; analgesic, antiinflammatory agent The present invention relates to new compounds of formula I, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of compounds of formula I.
US20120022121 Indoles, derivatives and analogs thereof and uses therefor Indole derivatives and analogous compounds and pharmaceutical compositions comprising the same are provided. Also provided are methods of using these compounds to inhibit tubulin polymerization in a cell associated with a proliferative disease or to treat cancer, metastatic cancer, resistant cancer or multidrug resistant cancer, including inter-alia: prostate cancer, breast cancer, melanoma, colon cancer and bladder cancer.
US20070140984 Functional powdery product The present invention has objects to provide a functional powdery product prepared by allowing carriers to support one or more members selected from vitamin glycosides, and to provide external dermatological agents having satisfactory usability, which contain the above functional powdery products and effectively exert the functions of vitamins. These objects are solved by providing a functional powdery product prepared by allowing carriers such as saccharides to support one or more members selected from vitamin glycosides, and by providing external dermatological agents incorporated with the functional powdery products.
US20120277187 Agent for Preventing Infection An agent for preventing an infection with an influenza virus or a food or drink for preventing infection with an influenza virus is provided. It is the agent for preventing an infection with an influenza virus and a food or drink for preventing an infection with an influenza virus, which comprises a fat globule membrane component as an active ingredient. It is the agent for preventing an infection with an influenza virus and a food or drink for preventing an infection with an influenza virus, which comprises a sphigosine-containing phospholipid and/or a derivative thereof, particularly sphingomyelin, as an active ingredient.
CN101048159A Pharmaceutical composition comprising a macrolide t-cell immunomodulator and anti-photoaging agent Compositions are provided comprising a macrolide T-cell immunomodulator or immunosuppressant agent, e.g. pimecrolimus, and at least one anti-photoaging agent such as a sunscreen, an anti-oxidant or a DNA-repair enzyme. They are useful in particular in the curative treatment or prevention of dermatological diseases and of conditions where it is desired to inhibit the skin aging effects of light radiation such as UV-A and UV-B light, e.g. development of skin cancer.
US20110238016 Drug delivery to a joint A drug delivery device may include a base to be percutaneously affixable in an attachment zone of a synovial joint and a sustained-release drug carrier coupled to the base. The drug delivery device may also include an access device to provide access to the attachment zone. The attachment zone may comprise a non-articulating portion of a bone and/or cartilage with the synovial joint and the drug carrier may elute the drug into the synovial fluid sufficient to sustain a therapeutically effective concentration of the drug in the synovial fluid for at least 8 hours.
US20100285128 Space filled drug release structure and method of manufacturing the same A space filled drug release structure and a method of manufacturing the same are disclosed. The structure is composed of a highly water-absorbing polymeric matrix and drug particles dispersed in the matrix. The matrix has pores and passages interconnecting the pores together. Because some water is present in the matrix, gastric acid can easily penetrate into the matrix to reach each drug particle. The surface of each drug particle is therefore possible to contact with the gastric acid. The drug releasing rate is therefore fast. Such structure is helpful for those drugs with low dissolution ability in the gastric acid.
CN101194925A Prescription of anticancer abolish poison medicament, preparing and taking method thereof The invention relates to a formula and a process for preparing and taking method of an anti-cancer and poison expelling medicament, the formula comprises vermillion 0.03g to 15g, dahurian angelica root 0.3g to 24g, bee honey 5g to 50g and green bean 50g to 500g. The process for preparing and taking method comprise first, picking foreign matters in thedahurian angelica root out, and washing and soaking the dahurian angelica root, taking the dahurian angelica root out and moistening, slightly sunning till ectoderm has no soapy feeling, grinding the dahurian angelica root to be standby after being moistened, being cut into pieces, and being dried, second, getting out vermillion which is manual made to mix with dahurian angelica root powder according to formula proportion, and adding adequate bee honey to reconcile to be pasty state for taking, third, cleaning the green bean to decoct soup on slow fire till the green bee is flowering to release sweetened bean paste out, fourth, according to sickness priority, focus position, ages, and physique and the other specific conditions, immediately drinking green bean soup when the soup is hot after oral administration according to adequate proportion of the formula, and the quantity of the green bee soup is according to comfortable feeling, and then covering quilts to keep warm and to sweat, gradually removing the quilts after whole body thoroughly sweats, and avoiding catching cold and wind chill.
CN101732613A Simple and quick-acting bone-setting medicament and preparation process thereof The invention discloses simple and quick-acting bone-setting medicinal powder, which comprises the following main components: natural silk, male hair, watermelon seeds, shallot roots, mature vinegar, honey and brown rice flour. Ten packets of the medicament comprises: 8g of natural silk, 8g of male hair, 6g of watermelon seeds, 6g of shallot roots, 30g of honey, 130g of mature vinegar and 190g of brown rice flour, wherein the watermelon seeds need to be stir-fried and the male hair and the natural silk need to be burned. The preparation process comprises the following steps of: burying the pre-baked watermelon seeds and the shallot roots under the brown rice flour; scattering silky hair carbon ash on the brown rice flour; stirring the mixed powder up and down by a shovel after the brown rice flour is completely cooled; after mixing the mixed powder relatively uniformly, rolling the composite powder by an iron roller and then sieving the composite powder through a fine basket; rolling the rough powder remained in the basket repeatedly until almost no dregs; and remaining more than 200g of fine powder to obtain the simple and quick-acting bone-setting medicinal powder. Due to the adoption of the technical scheme, the preparation process is simple, the materials are convenient to obtain; and the prepared medicinal powder has the advantages of good curative effect and low cost.
CN101744780A Clopidogrel dispersible tablet and preparation method thereof The invention discloses a clopidogrel dispersible tablet and a preparation method thereof, in particular relates to a clopidogrel hydrogensulfate preparation and a preparation method thereof. The clopidogrel hydrogensulfate preparation is used for curing various thrombosis induced by platelet aggregation. The clopidogrel hydrogensulfate preparation and the preparation method with short disintegration time, excellent dispersed state, quick drug dissolution and convenience and flexibility of taking have the characteristics of improving the medication compliance of the patients, ensuring the therapeutic effect of the drug and the like.
CN101317836A Application of (3aR,5R,11bR)-3,3a,5,11b-tetrahydro-7-hydroxyl-5-methyl-2H-furo[3,2-b]naphtho[2,3-d]pyran -2,6,11-trione The present invention pertains to the field of medical technique, in particular relates to application of (3aR, 5R, 11bR)-3, 3a, 5, 11b-tetrahydro-7-hydroxy-5-methyl-2H-furan (3, 2-b) naphtho (2, 3-d) pyrane-2, 6, 11-triketone, namely the application of the compound to preparation of antitumor antibiotic. The compound of the present invention has very strong cytotoxicity with an average median lethal concentration of 0.06Mug/mL in the 37 pieces of tumor cells in human body and can be taken as the strong active compound of antineoplastic. The compoumd has inhibitory action on a great variety of tumor cells in human body, and can be taken as clinical medicine or lead compound.
WO2013178065A1 Amino acid copper complex with effects of preventing alopecia, growing hair and protecting skin, preparation method and application Disclosed are an amino acid copper complex with the effects of preventing alopecia, growing hair and protecting skin, a preparation method and application. The amino acid copper complex is obtained by complexing divalent copper ions with amino acid having an amino acid structure (1) and/or an amino acid structure (2). The amino acid copper complex has the same effects as copper polypeptide, has the effect of repairing skin, preventing alopecia and growing hair, can be used as a substitute product of expensive copper polypeptide, and can be used as alopecia prevention, hair growth or skin care products. The preparation method is simple, is low in cost, and can meet the demand of people on alopecia prevention products, and relieve the trouble brought by alopecia for modern people.
US20080033022 Inhibitors of c-Jun N-terminal kinases (JNK) The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
US6888016 For therapy of insulin resistance; for stimulating the glucose up-take in adipocytes Our invention concerns a mixture of CLA glycerides, and/or CLA-fatty acids and or CLA-alkyl esters and another component, wherein the other component (=component A) is selected for its capacity to alleviate problems related to insulin resistance in mammals, using CLA rich diets and/or foods and/or food supplements using an appropriate in vitro test so that in at least one step of the in vitro test, as described in the text, an improvement in test results is obtained of at least 4% by the blend of the CLA derivative and component A when compared to the CLA derivative only. The inventon further concerns CLA rich dietic food, food supplements and foods containing the combination of CLA and component A as defined, while also the use of this combination for achieving an alleviation of insulin resistance is part of the invention.
CN103142642A Calcitriol and calcium carbonate suspension granule and preparation method thereof The invention relates to a calcitriol and calcium carbonate suspension granule and a preparation method thereof. The suspension granule is prepared from the following ingredients in percentage by weight: 0.0005% of calcitriol, 5-10% of calcium carbonate, 2.0-4.0% of meglumine, 1.2-1.8% of polyethylene glycol 400, 12-18% of polyethylene glycol 6000, 45-75% of filler, 5.0-10.0% of disintegrant and an appropriate amount of binder. According to the suspension granule, the content of calcitriol is remarkably increased, so that the drug dosage is reduced; and the stability of calcitriol to light and air is improved, and the bioavailability of calcitriol is also remarkably improved.
CN101550120A Effective component of artemisia leaves and preparation method thereof The invention relates to an effective component of artemisia leaves as well as a preparation method and an application thereof. The preparation process of the effective component comprises the following steps: (1 )a mixture of ethyl acetate and ethanol is used as a solvent to extract the artemisia leaves; (2) an extracting solution is processed by chromatography through a chromatographic column to obtain an eluent; (3) the eluent is eluted by prepared liquid chromatogram gradient and is collected for 4.0-8.0 minutes, 8.0-10.0 minutes, 16.0-20.0 minutes, 20.0-24.0 minutes, 24.0-28.0 minutes, 28.0-32.0 minutes and 36.0-40.0 minutes to obtain the effective component by taking water and acetonitrile as flow phases.
CN102988277A Ointment for treating dermatoses such as cutaneous wart, onychomycosis and callus The invention discloses an ointment for treating dermatoses such as cutaneous wart, onychomycosis and callus, belonging to the field of medicaments for treating the dermatoses. The ointment comprises the following components in percentage by weight: 25-30 percent of lactic acid, 25-30 percent of salicylic acid, 25-30 percent of wool fat and 12-15 percent of petrolatum. The ointment disclosed by the invention has the characteristics of definite curative effect, high effect taking speed, convenience in use, low cost, and good patient compliance.
CN102093340A Preparation method and application of 2-methylindazole derivatives The invention belongs to the field of drugs for treating angiogenesis-related diseases and provides 2-methylindazole derivatives with the structure in the general formula K or pharmaceutically acceptable salts thereof, wherein in the formula, R1 is hydrogen, C1-C6 alkyls or mono-substituted or multi-substituted C1-C6 alkyls; R2 is phenyl, nitrogen atom-containing heteroaryl, phenyl mono-substituted or multi-substituted by halogen, hydroxyl, carboxyl, amino, nitryl, nitrile group, ester group, C1-C6 alkylthio groups, C1-C6 alkoxy, halogen-substituted C1-C6 alkoxy and C3-C6 cycloalkyl, or nitrogen atom-containing heteroaryl mono-substituted or multi-substituted by halogen, hydroxyl, carboxyl, amino, nitryl, nitrile group, ester group, C1-C6 alkylthio groups, C1-C6 alkoxy, halogen-substituted C1-C6 alkoxy and C3-C6 cycloalkyl. The invention also provides applications of the compounds or pharmaceutically acceptable salts thereof as drugs, especially anti-tumor drugs.
EP2205561A2 Substituted piperazines and piperidines as modulators of the neuropeptide y2 receptor The invention relates to compound of the formula (I): wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.
WO2010110374A1 Agent for enhancing hypoglycemic activity An agent for enhancing an hypoglycemic activity, which comprises an α-glucosidase inhibitor containing at least one bacterium selected from the group consisting of a bifidus bacterium, a lactic acid bacterium, a saccharification bacterium and a butyric acid bacterium.
CN101314584A HGF/c-Met signalling channel restrainer, preparation method and application thereof The invention relates to 2-indolone derivative series (formula I), medicinal salts thereof, isomers thereof, hydrates thereof or solvates thereof and the preparation method thereof; and the invention also relates to a pharmaceutical composition containing the same with an effective dosage and the application thereof in prevention and treatment of tumor diseases by blocking the HGF/c-Met signal channels.
WO2014043257A1 Treatment for vitiligo Compounds I and II, as well as prodrugs, hydrates, solvates, N-oxides, salts and pharmaceutical compositions containing them, are useful for treating vitiligo. In certain embodiments, the compounds are provided in topical compositions. (The chemical formulas should be inserted here.)
CN103304513A One-class 1,2-benzothiazine compound as well as preparation method and application thereof The invention relates to the field of medicines, and in particular relates to a 1,2-benzothiazine compound (I) for treating tumors, a preparation method and a medicine composition with the compound. The definitions of R and Ar are as shown in the specification. The pharmacodynamic test shows that the compound has the remarkable anti-tumor function, and the tumor which can be treated by the compound is preferably small cell lung cancer, non-small cell lung cancer, liver cancer, colon cancer, carcinoma of the rectum, stomach cancer, breast cancer, skin cancer or prostate cancer.
US20100210661 Stat3/5 activation inhibitor An object of the present invention is to provide a STAT3/5 activation inhibitor. The present invention provides a STAT3/5 activation inhibitor containing an aromatic compound represented by the general formula or a salt thereof as an active ingredient: wherein X1 represents a nitrogen atom or a group —CH═, R1 represents a group —Z—R6, in which Z represents a group —CO—, a group —CH(OH)— or the like, R6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents a group wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl lower alkyl group or the like.
US7154001 Formate salt of O-desmethyl-venlafaxine A novel salt of O-desmethylvenlafaxine, O-desmethylvenlafaxine formate, is provided. Pharmaceutical compositions, dosage forms and methods of use are also provided.
WO2006034094A1 Crystalline form 1 of atrasentan hxdrochloride Atrasentan Hydrochloride Crystalline Form 1, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
EP2081590A2 Cancer stem cell-targeted cancer therapy The present invention provides methods for stabilizing, reducing or eliminating cancer cells. In particular, the present invention provides prophylactically and/or therapeutically effective regimens for the prevention, treatment and/or management of cancer, the regimens comprising administering one or more cancer therapies to a subject to reduce a cancer cell population. The therapy(ies) in the prophylactically and/or therapeutically effective regimen can be administered at a lower dose than currently used or known to one of skill in the art and/or for a longer period of time and/or more frequently than currently administered or known to one of skill in the art.
EP2358669A2 Alpha-keto peracids and methods for producing and using the same The present invention provides alpha-keto peracids and methods for producing and using the same. In particular, alpha-keto peracids are useful as antimicrobial agents.
US7951820 Triazole compounds useful as protein kinase inhibitors This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.
CN102218078A Rifaximin suspension containing montmorillonite and preparation method thereof The invention discloses rifaximin suspension containing montmorillonite, which belongs to the field of veterinary preparations. The rifaximin suspension comprises the following components by weight percent: 5-15% of rifaximin, 7.5-22.5% of the montmorillonite, 0.5-2% of suspending agent, 0.2-1% of surface active agent, 0.2-1% of deflocculating agent and the balance of water. The invention further discloses a preparation method of the rifaximin suspension, which comprises the following steps: adding the suspending agent, the surface active agent and the deflocculating agent into the water according to proportion, uniformly mixing and performing water bathing for 1-3 hours at the temperature of 65 DEG C; further adding the rifaximin and the montmorillonite into a stirrer for stirring; and adding the water to volume, homogenizing and sterilizing. The rifaximin in the rifaximin suspension is small in particle size, the release amount and the release speed of active ingredients are greatly improved, and the bioavailability of the rifaximin is improved; secondly, the mortality rate of livestock and poultry with diseases caused by diarrhea can be reduced; in addition, the rifaximin suspension is good in stability and suitable for long-term preservation.
CN102988452A Externally applied plaster and its preparation method The invention discloses an externally applied plaster. The externally applied plaster is prepared from the following raw materials, by weight, 0.5 parts of musk, 12 parts of dahurian angelica root, 0.2 parts of Calculus Bovis, 10 parts of Boswellia carteri, 20 parts of stalactite, 100 parts of red lead and 650 parts of sesame oil. The preparation method of the externally applied plaster comprises the following steps: boiling the sesame oil, adding the dahurian angelica root and the stalactite, decocting until the dahurian angelica root is black, and taking out the dahurian angelica root and the stalactite; decocting by a medium fire, adding the Calculus Bovis, and decocting for a moment; and slowly adding the Boswellia carteri, the musk and the fine powder of the red lead under fast stirring. The externally applied plaster has the efficacies of anti-inflammation, detumescence, blood circulation promoting, vein relaxing, pain relieving, bleeding stopping, necrotic tissue removing, flesh engendering and the like after the use of patients, so the externally applied plaster can be widely used for treating sharp instrument injuries, sprain and contusion, burns, frostbites, pains, gangrenes, furuncles, malignant boil and ulcers.
WO2007061237A1 Composition for anti-inflammation The present invention provides a composition for anti-inflammation comprising one or more ingredients of 8 -hydroxy guano sine (oh8G) and 8-hydroxydeoxyguanosine (oh8dG) as active ingredients. The present composition comprising one or more ingredients of oh8G and oh8dG suppresses the activity of Rac 2 of macrophage, thereby suppressing the activity of NADPH oxidase and also ROS production. Furthermore, the composition of the present invention suppresses the rising of blood concentration of pro-inflammatory cytokine induced by LPS, the increasing of MPO activity and Rac 2 activity, and the mortality of mouse due to LPS. Thus, the composition for anti-inflammation of the present invention can be used for treating various inflammatory diseases such as rheumatic arthritis, Lupus ethrythematosus, multiple scleroderma, adult respiratory distress syndrome (ARDS), etc., as an anti-inflammatory agent.
CA2322195C Novel diphenyl-substituted 5-ring-heterocycles, method for producing them and their use as medicaments The invention relates to new diphenyl-substituted 5-ring heterocycles of general formula (I) wherein A, X and the groups R1, R2, R3, R4 and R5 are defined as in the claims, processes for preparing them and their use as pharmaceutical compositions.
WO2012075257A2 Compositions for oral and nasal hygiene The present disclosure encompasses pharmaceutically acceptable antimicrobial compositions of an amount of levulinic acid and sodium dodecyl sulfate effective in reducing the microbial population of an internal cranial cavity of a recipient human or animal subject. The disclosure also provides methods for reducing a microbial population of an internal cranial cavity of a recipient human or animal comprising contacting the oral cavity or sinuses of the subject with a composition comprising between about 0.5% to about 5% by weight per volume of levulinic acid and between about 0.05% to about 2% by weight per volume of sodium dodecyl sulfate (SDS) and for a period effective in reducing a microbial population of the oral cavity.
DE102010062544A1 New substituted 1-benzylcycloalkylcarboxylic acid compounds are soluble guanylate cyclase activators useful to treat and/or prevent e.g. heart failure, angina pectoris, hypertension, pulmonary hypertension and vascular disease Substituted 1-benzylcycloalkylcarboxylic acid compounds (I) and their salts, solvates or solvates of the salts, are new. Substituted 1-benzylcycloalkylcarboxylic acid compounds of formula (I) and their salts, solvates or solvates of the salts, are new. R1aR1bC : cyclopropan-1,1-yl, 2,2-difluoro-cyclopropan-1,1-yl or cyclobutan-1,1-yl; R 2> : H, CH 3, C 2H 5, vinyl, OH, CH 3O, trideuteromethoxy, CF 3O, C 2H 5O or cyclopropyloxy; R 3> : H, CH 3, C 2H 5, isopropyl or cyclopropyl; R 4> : H, F, Cl, Br, CN, CH 3, CF 3, C 2H 5, isopropyl, cyclopropyl, cyclobutyl, CH 3O or CF 3O; R 5>, R 6> : H, F, Cl, CH 3, CF 3or CF 3O; either R7a : CH 3or C 2H 5; and R7b : CF 3; or R7aRbC : cyclopentane, 1,1-difluoro-cyclopentan-2-yl or 1,1-difluoro-cyclopentan-3-yl; R 8> : 1-4C-alkyl, 2-4C-alkenyl (both optionally substituted by 2 or 3 F), cyclopropyl or cyclobutyl (both optionally substituted by up to 2 F), F, Cl, Br, nitro, CN, CF 3O, acetyl or 2-cyanovinyl; and R 9> : H, F, Cl, CH 3, CF 3, C 2H 5, CH 3O or CF 3O. Independent claims are included for: (1) the preparation of (I); and (2) a medicament comprising (I) in combination with one or more inert, non-toxic auxiliary agent. [Image] - ACTIVITY : Cardiant; Antianginal; Hypotensive; Respiratory-Gen.; Cerebroprotective; Vasotropic; Thrombolytic; Antiarteriosclerotic; Ophthalmological; Auditory; Neuroprotective; Cardiovascular-Gen.; Antiulcer; Dermatological; Fungicide; Antirheumatic; Nephrotropic; Antianemic; Osteopathic; Metabolic; Uropathic; Cytostatic; Endocrine-Gen.; Nootropic; Antiparkinsonian; Anticonvulsant; Tranquilizer; Antidepressant; Hypnotic; Antiaddictive; Analgesic; Antibacterial; Immunosuppressive; Antiinflammatory; Antiarthritic; Vulnerary. - MECHANISM OF ACTION : Soluble guanylate cyclase activator. The ability of (I) to activate soluble guanylate cyclase was tested Chinese hamster ovary cell. The results showed that 1-(4-fluoro-3-{[(2S,3R)-4,4,4-trifluoro-2-(4-isop ropylphenyl)-3-methylbutanoyl]amino}-benzyl)cyclopropane carboxylic acid exhibited a minimal effective concentration value of 0.1 nM.
US20050209206 Pharmaceutical formulation comprising an androstane derivative and a solubilising agent in an aqueous liquid carrier A pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) a glucocorticoid of formula (I) wherein R represents a 5 membered heterocyclic aromatic ring containing 1 to 3 heteroatoms selected from O, N and S, optionally substituted by one or more methyl or halogen atoms or a solvate thereof, as a medicament; and (b) a solubilising agent for assisting the solubilisation of the medicament in the aqueous carrier liquid.
US20110082187 Markers and methods relating to the assessment of alzheimer's disease Use of clusterin as a biomarker of Alzheimer's disease (AD), particularly methods and compositions for detection of clusterin in a biological sample and assessment of in vivo pathology, disease severity and rate of clinical progression in a subject having or suspected of having AD.
EP1131077B1 Bicarbonate-based solution in two parts for peritoneal dialysis or as a substitution solution in continuous renal replacement therapy The present invention provides devices and methods for stabilizing bicarbonate-based solutions for peritoneal dialysis or hemofiltration. The bicarbonate-based solutions of the present invention are formulated and stored in at least two parts - an alkaline bicarbonate concentrate and an acidic concentrate. The alkaline bicarbonate concentrate is adjusted to have a pH of about 8.6 to 10.0. The acidic concentrate is adjusted to have a stable, acidic pH ranging from about 1.0 to 3.0. Upon mixing, although some variation in the pH of the mixed bicarbonate solution exists, the inventors have discovered that with the appropriate selection of the parameters of the concentrates, the pH of the mixed solution is always within an acceptable physiological range.
CN101371840B Novel use of vinetine and analogue thereof in preparing medicine for preventing and/or treating leukemia The invention discloses new applications of oxyacanthine and oxyacanthine analogue. The invention refers to the applications of oxyacanthine, expressed by a formula (I), and oxyacanthine analogue or pharmaceutically acceptable salt thereof in the preparation of medicament for inhibiting of the proliferation of eukaryote tumor cells and medicament for preventing and/or treating tumor. Oxyacanthineexpressed by formula (I) and oxyacanthine analogue or the pharmaceutically acceptable salt thereof can combine with G-quadruplex DNA to increase the stability of G-quadruplex DNA, so as to competitively inhibit the combination of a telomerase and a telomere, restrain the activity of the telomerase, weaken the proliferation capability of cells of the telomerase, control the extension of the telomere and accelerate the apoptosis of telomere cells. Vitro cancer cell proliferation experiments prove that: oxyacanthine has comparatively good inhibition effect on human leukemia cell system HL-60, human gastric cancer cell system BGC-823, human liver cancer system Bel-7402 and human nasopharyngeal cancer system KB, and the inhibition rate to the cancer cells can reach over 80 percent when the medical concentration of oxyacanthine is higher than 25muM.
CN101204355A Application of polyenic carboxylic Ca in health-care and beauty field The invention relates to a method for applying the polyene acid calcium in the field of the medical treatment and cosmetology. At present, the polyene acid calcium is never applied in the field of the medical treatment and cosmetology. The invention consists of the polyene acid calcium, the glycerin, the octadecyl alcohol, the monoglyceride, the white mineral oil, the albolene, the P20 emulgator, the propylene glycol, the preservative K400 and the essence and water. The polyene acid calcium is calendic acid calcium, linolic acid calcium or octadecenoic acid calcium. The invention has the efficacies of resisting crease, whelks, acnes, stains and dead skins, reducing sweat pores, removing scars caused by the whelks, sunburn, graze, skin injury, die burn and frostbite and preventing freezing, framing, aging, and sunburn, repairing and regenerating skins and repairing the damaged skins due to diversified reasons. The invention has the advantages of remarkable medical efficacy, low production cost, no toxic and side effects, safety and reliability and easy popularization.
CN102225057A Application of oxymatrine-containing composition in preparing inhalant antiasthmatic medicament The invention discloses an application of an oxymatrine-containing composition in preparing an inhalant antiasthmatic medicament; the dosage form of the inhalant medicament is an inhalant solution formulation or an inhalant powder formulation; the purity of oxymatrine is above 90%; and the pharmaceutical excipient is any one or more than one of a solvent, a cosolvent, a surfactant, a flavouring or a carrier. According to the invention, the oxymatrine is a monomer component with high purity; aiming at symptomatic characteristics of asthma, especially targeting bitter receptors in respiratory tract, the oxymatrine can directly enter the respiratory tract and the lung after being inhaled, and is rapidly absorbed so as to alleviate symptoms of asthmatic patients, enhance efficacy, and improve the compliance of medication for patients. The composition has higher efficacy and less side-effect. Preparing an inhalant antiasthmatic medicament by the oxymatrine-containing composition is a special new application of the oxymatrine-containing composition in relieving asthma, and the medicament is a new preparation. The medicament has no toxicity, is low in price and low in cost, and has wide market prospects.
EP2520304A1 Ceramide production enhancer and moisturizing agent A ceramide production enhancer and a moisturizer containing, as an active ingredient, an extract of at least one plant selected from the group consisting of Chenopodium hybridum, Melia toosendan, Indigofera tinctoria, Cirsium japonicum, Catalpa ovata, and Tagetes erecta, or a compound represented by the following Formula (1): wherein, R represents an acyl group having 1 to 5 carbon atom(s).
US7087641 4β-1″-[(2″-substituted benzoyl) anilino]podophyllotoxin analogues useful as anticancer agents The present invention provides a new class of compounds 4β-1″-[{2″-benzoyl substituted}anilino] podophyllotoxin exhibiting anti cancer activity and a process for preparing the same.
CA2396145C Osmotic device containing pseudoephedrine and an h1 antagonist The present invention provides an osmotic device containing controlled release pseudoephedrine in the core in combi-nation with a rapid release H1 antagonist in an external coat. A wide range of H1 antagonist antihistamines, especially fexofenadine, can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray coated rather than compression coated onto the device. The device with spray coated external core is smaller and easier to swallow than the similar device having a compression coated external coat. The device is useful for the treatment of respiratory congestion related disorders and allergy related disorders. The present devices provide PS and an H1 antagonist according to specific release profiles in combination with specific formulations.
CN101502510A Medicament composition for treating colpitis symptoms and preparation method thereof The invention relates to a drug combination for curing the inflammation of vagina, which adopts the form of a foaming agent, in particular to a foaming agent with the principle agents being metronidazole, clotrimazole and chlorhexidine acetate. The drug combination has the advantages of even distribution, wide coating area and better effect in the vagina by adopting the form, and meanwhile, the drug combination feels more comfortable and has stronger retention property than other forms. In the formula of the foaming agent, the drug combination can permeate into the mucosal folds of the vagina rapidly and effectively by dispersing atomizing particles with the particle diameter being a few micrometers in a foaming manner under the action of pressure; the drug combination has higher absorption rate than the spraying agent with water being the only solvent with the assistance from various fat-soluble auxiliary materials; the drug contamination and the cross contamination are avoided during the administration; the invention has the advantages that the curative effect is fully produced, the administration is sanitary, convenient, safe and reliable without causing the foreign body sensation, and the drug combination is easily accepted by patients; and the invention further has the advantages of drug stability, form stability and long effective duration.
US7628984 Micronutrient formulations for pulmonary and heart health A heart and pulmonry health micronutrient formulation is provided and the formulation comprises dietary antioxidants and endogenous antioxidants, and the formulation comprising dietary micronutrients and endogenous antioxidants, the dietary antioxidants are selected from a group consisting essentially of Vitamin A (Palmitate), Vitamin E, Vitamin C, Vitamin D3 (Cholecalciferol), B Vitamins, Biotin, Pantothenic Acid (as D-Calcium Pantothenate), Calcium Citrate, Magnesium Citrate, Zinc Glycinate, Selenium (Seleno-L-Methionine), Chromium (as Chromium Picolinate), Mixed Carotenoids and mixtures thereof, and the endogenous antioxidants are selected from a group consisting essentially of N-Acetyl Cysteine (NAC), Coenzyme Q10, R-alpha Lipoic Acid, Omega-3 fatty Acid, and L-Carnitine and mixtures thereof.
CN101259123A Application of isoforskolin and its analogue in preventing and controlling lung injury The invention relates to novel applications of isoforskolin and analogous compounds thereof, in particular to the applications in the prevention and/or treatment of lung injury; the lung injury mainly includes acute lung injury and lung injury caused by such factors as smoking, surgery, wound, blood transfusion, mechanical ventilation, ischemia, ischemia reperfusion, and diseases. The adult dosage of the isoforskolin and analogous compounds thereof is 60-120mg every day, and the delivery forms include a peroral form, a spraying form and an injection form. The isoforskolin and analogous compounds thereof of the invention can be prepared into various peroral dosage forms such as tablets, buccal tablets, capsules, granules, and oral liquid, and can also be prepared into such dosage forms as injection liquid, aerosol, and emplastrum. The invention is a discovery of novel medical and health care applications for given compounds, isoforskolin and analogous compounds, and a development of a novel application field. The isoforskolin and analogous compounds of the invention can be independently used as medicines or effective health care components, compatible with other non-repulsive components and can be prepared into medicaments or health products with corresponding dosage forms.
CN1843441A Rheumatism-eliminating collaterals-dredging externally applied plaster The invention relates to a pharmaceutical composition for treating arthralgia syndrome and process for preparation, wherein the raw materials include Sichuan aconite root, Kusnezoff monkshood root, pinellia tuber, rhubarb horsetails, pawpaw, notopterygium root, pubescent angelica root, radix paeoniae rubrathe, jack-in-the-pulpit tuber, datura flower, seed of nuxvomica, white mustard seed, achyranthes and cyathula root, safflower, camphor, asaryl, musk and baras camphor.
WO2011158248A2 Process for preparation of posaconazole and crystalline polymorphic form v of posaconazole Disclosed are a process for preparation of an antifungal agent posaconazole and crystalline polymorphic form V of antifungal agent posaconazole.
CN1907271A Selegilne and/or chlorhydric acid selegilne paste matrix and preparation method for said paste The invention discloses a Slagilan and or alcaine Slagilan attaching agent base and preparing method, which comprises the following parts: Slagilan and or alcaine Slagilan, adhesive and organic solvent. The preparing method comprises the following steps: (1) coating compound of raw materials on the back lining evenly; (2) drying; covering the protective film on the other surface of attaching base to obtain the product.
CN101732303A Medicinal use of leonurine for menopause disease The invention relates to medicinal use of leonurine for menopause disease, and in particular provides the medicinal use of the leonurine or pharmaceutical salts thereof for preventing or treating menopause syndrome and menopause syndrome related diseases.
CN103479613A Application of fluoro taxane derivative in preparation of liver cancer treating drugs The invention belongs to the field of medicinal chemistry, and relates to an application of a fluoro taxane derivative represented by the formula (1) in preparation of liver cancer treating drugs, wherein R1 is hydrogen or fluorine, R2 is hydrogen or fluorine, R3 is hydrogen or fluorine, R4 is hydrogen or fluorine, and R5 is hydrogen or fluorine. In vitro pharmacological studies show that the fluoro taxane derivative has an obvious anti-tumor effect and a good dose-dependent relationship; test results related to human cancer cytotoxic activity show that the anti-tumor effect of the fluoro taxane derivative is equal to that of docetaxel activity, even better than that of docetaxel; and in vivo pharmacological experiment results show that the fluoro taxane derivative can inhibit division and proliferation of liver cancer cells, and has an obvious effect of treating liver cancer. The fluoro taxane derivative can further be made into liver cancer treating medicinal preparations with medicinal carriers.
EP1416926A4 Zinc containing compositions for anti-viral use One aspect of the invention relates to anti-viral composition containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients such as at least one analgesic, at least one hydrocarbyl containing compound, and water). Another aspect of the invention relates to a method of treating lesionous symptoms of a viral infection involving applying an effective amount of the zinc containing anti-viral composition to the lesions.
CN103193788A Lycorine alkaline compound with neuroprotective effect The invention belongs to the technical field of medicine, relates to amaryllidaceae alkaloids, and particularly provides a lycorine alkaline compound extracted from hybridized lycoris (a hybrid product of L. aurea and L. radiata). The compound has a protective effect on nerve cells, has prevention and treatment effects on Alzheimer's disease, and can be used for preparation of neuroprotective agents and drugs for preventing Alzheimer's disease.
US20110305770 Releasable polymeric lipids for nucleic acids delivery system The present invention relates to polymer conjugated releasable lipids and nanoparticle compositions containing the same for the delivery of nucleic acids and methods of modulating gene expression using the same. In particular, this invention relates to releasable polymeric lipids containing an acid-labile linker based on a ketal or acetal-containing linker, or an imine-containing linker.
CN1961957A Anti-aging colon absorption preparation The invention discloses an antisenescence colon absorbing agent comprising the following constituents (by weight percent): collagen powder 30-80%, grape seed extract 1-10%, vitamin C 1-20%, vitamin E 0-20%, calcium carbonate or calcium acetate or calcium gluconae or sclerotin calcium phosphate silicate or amino acid chelated calcium or calcium lactate or calcium citrate 0-50%, chitosan or chitosan salts or chitosan derivatives 9-15%, crystalline cellulose or sodium carboxymethylstarch or low substituted methylcellulose propylene glycol ether 1-50%, the agent can improve absorption of collagen.
EP2493463A1 Use of menthyl ethers as anti-bacterial, anti-mycotic or anti-viral active substances The invention relates to the use of menthyl ethers with a structure (I), in which R represents a branched or unbranched alkyl group, optionally monosubstituted or polysubstituted with hydroxy groups and comprising up to 10 carbon atoms, as anti-bacterial, anti-mycotic or anti-viral active substances.
US20080108677 Thioxothiazolidinone Compounds For Use As Pharmaceuticals The present invention relates to thioxothiazolidinone compounds for use as pharmaceuticals, to pharmaceutical compositions comprising these compounds, and to the use of said small-molecule compounds for the manufacture of pharmaceutical compositions for the treatment of conditions dependent on leukocyte cell migration, such as leukaemia and inflammatory diseases. Said compounds inhibit leukaemia cell migration by stabilizing the active conformation of the αM integrin I domain.
US20140287028 Use of Chemotherapeutic Agents The use of chemotherapeutic agents for the preparation of a medicament for the topical and/or local treatment of diseases caused by bacteria and/or for prophylaxis in humans or animals.
US20100184771 Bicyclic Heterocyclic Compound A compound represented by the formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof: wherein X1 represents N and X2 represents C, or X1 represents C and X2 represents N; Y1 represents CR4 or N; Y2 represents CH or N; wherein both Y1 and Y2 do not represent N at the same time; R1 represents (1) C3-10 branched alkyl which may be substituted or (2) —(CH2)m—NR5R6; R2, R3, and R4 each independently represent H, C1-4 alkyl, a halo-substituted C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, or the like; R5 and R6 each independently represent C1-6 alkyl which may be substituted, or R5 represents H, and R6 represents C3-6 branched alkyl which may be substituted; and Ar represents an aromatic ring which may be substituted, is useful as a pharmacologically active ingredient having a CRF antagonistic activity in preventing and/or treating neuropsychiatric diseases, diseases of peripheral organs or the like.
US20090042971 Method of using low-dose doxepin for the improvement of sleep Methods of preventing early awakenings, and improving sleep efficiency in hours 7 and 8 of a period of sleep, by administration of low doses of doxepin (e.g., 1-6 mg).
CN103483460A Preparation method of ulva fasciata delile sulfated polysaccharide with anti-tumor activity The invention discloses a preparation method of an ulva fasciata delile sulfated polysaccharide with anti-tumor activity. The preparation method comprises the following steps of crushing and ultrasonically extracting ulva fasciata delile by water to prepare a crude polysaccharide through alcohol precipitation; carrying out depigmentation deproteinization by using a radial-flow chromatographic column which is filled with weakly basic anion exchange resin; carrying out ultrafiltration separation according to molecular weight after elution; and taking and adding an ulva fasciata delile polysaccharide compound with molecular weight of 10 KD to 30 KD into the radial-flow chromatographic column which is filled with DEAE (Diethyl Aminoethanol) sepharose gel for enriching and purifying, wherein the prepared polysaccharide with average molecular weight of 20 KD has remarkable antitumor activity.
WO2007132292A3 Therapy for alzheimer's disease The present invention relates to newly identified methods and compositions for modulating the cellular processing of beta-amyloid precursor protein ('APP') and for the prevention or treatment of diseases associated with abnormal APP processing, such as Alzheimer's disease ('AD'). The invention also relates the identification of molecular pathways heretofore unknown to be involved in APP processing. The invention also relates to the prevention or treatment of AD disease symptoms using medicaments that modify the activity of novel molecular targets involved in APP processing.
WO2013127268A1 Amido-benzyl sulfone and sulfonamide derivatives Disclosed are certain amido-benzyl sulfone and sulfonamide compounds, pharmaceutical compositions comprising such compounds, land methods of treatment using such compounds.
WO2005094823A1 Flt-3 INHIBITOR A Fms-like tyrosinkinase 3 (Flt-3) inhibitor which contains as an active ingredient either an indazole derivative represented by the formula (I) [wherein X represents a single bond, (CH2)n2CH=CH(CH2)n3 (wherein n2 and n3 are the same or different and each is an integer of 0 to 4), etc.; R1 represents (un)substituted aryl or an (un)substituted heterocyclic group; and R2A, R2B, R2C, and R2D are the same or different and each represents hydrogen, halogeno, (un)substituted lower alkyl, etc.; provided that not all of R2A, R2B, R2C, and R2D are hydrogen] or a pharmacologically acceptable salt thereof. (I)
WO2011076734A1 Compounds, pharmaceutical composition and methods for use in treating inflammatory diseases The present invention relates to compounds of formula (I) (I) useful in treating and/or preventing inflammatory diseases.
CN101104646A Preparation method for eucheuma gelatinae polysaccharide selenide and application The invention discloses a novel preparation method of eucheuma gelatinae polysaccharide selenide. The selenylation of the eucheuma gelatinae polysaccharide is processed by sodium selenite being catalyzed by dilute nitric acid. The preparation method is simple, environment protecting, convenient and economic. The production shows higher biological activity, which can be applied widely in preparing the drug for inhibiting cancer cells, and has wide application prospect.
US20110060036 Branched Multifunctional Nanoparticle Conjugates And Their Use Disclosed herein are compounds and compositions including a polyglycerol nanocarrier, a therapeutic agent or imaging agent, and optionally a targeting agent. In certain aspects the disclosed compounds include biocompatible hyperbranched polymer nanocarriers. Such compounds and compositions are useful for the targeted delivery of antitumor agents and imaging agents to tumors in vivo. Methods are also disclosed for detecting and treating such tumors.
WO2007079239A3 Bicyclic nitrogen compounds as modulators of ghrelin receptor and uses thereof Disclosed herein are compounds of Formula I as defined herein, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, that modulates the activity of a ghrelin receptor. Disclosed herein are also methods of treating diseases or conditions that comprise administering to a subject in need thereof a therapeutically effective amount of a compound of Formula I.
EP2636404A2 Methods of Treating Non-Alcoholic Steatohepatitis (Nash) Using Cysteamine Products The disclosure relates, in general, to treatment of fatty liver disorders comprising administering compositions comprising cysteamine products. The disclosure provides administration of enterically coated cysteamine compositions to treat fatty liver disorders, such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH).
WO2007057768A3 Sulfonyl derivatives The present invention relates to compounds, pharmaceutical compositions comprising these compounds and methods for treating a condition that is mediated by the modulation of the 11-β-hsd-1 enzyme.
US20120142677 Pyrrolidine Compounds Which Modulate The CB2 Receptor Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. (I)
CN102973588A Application of carrageenan in preparing medicament for treating diabetes mellitus The invention discloses novel application of carrageenan in preparing a medicament for treating diabetes mellitus. The medicament can protect a body from insulin resistance due to chronic inflammation caused by activated macrophage generated by fat and other reasons, so that attack or symptom worsening of diabetes mellitus can be inhibited. Carrageenan has good curative effect in a high glucose and lysophosphatidylcholine induced animal model; and the medicaments used in the application can be easily acquired, low in price and stable in properties, are convenient to store and transport, and have wide application prospect.
CN102961349A Acetaminophen sustained-release dropping pill and preparation method thereof The invention relates to an analgesic, antipyretic, sedative acetaminophen sustained-release dropping pill and a preparation method thereof. The invention aims to solve the defects of other oral preparations, and provides the acetaminophen sustained-release dropping pill, which has advantages of high bioavailability, rapid effectiveness, long action time, low frequency of drug taking, convenient usage, toxicity, less side or toxic effect, convenient storage and transportation, and suitability for oral administration, and the preparation method thereof.
WO2008014299A3 Use of an alpha2-agonist composition for the treatment of hyperlipidemia Disclosed is the use of an agonist of the alpha2B and/or alρha2C adrenergic receptor subtypes that lacks (a) significant alpha2A adrenergic receptor activity or (b) significant alphalA adrenergic receptor activity, or that lacks both (a) and (b) for treating hyperglycemia or hyperlipidemia.
CN101787008A N-acetyl neuraminic acid compounds, medicine compositions thereof and preparation methods and purposes thereof The invention discloses N-acetyl neuraminic acid compounds shown as the following general formula, medicine compositions thereof and preparation methods and purposes thereof. The compounds can inhibite surface neuraminidase of influenza viruses, thereby resisting the influenza viruses, in particular treating the infections of the influenza viruses resistant to other influenza-resistant medicaments, such as Zanamivir, Oseltamivir and the like.
WO2011060112A1 Deuterated tyrosine kinase inhibitors Compounds of Formula I, as shown below and defined herein: enriched in deuterium, and pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by IGF-1 R and/or IR.
US20090137554 1,4,5,6-TETRAHYDRO -PYRROLO[2,3-d]AZEPINES AND -IMIDAZO[4,5-d]AZEPINES AS MODULATORS OF NUCLEAR RECEPTOR ACTIVITY Disclosed are chemical entities including compounds of Formula I and pharmaceutically acceptable salts thereof, wherein X is chosen from CN, CF3, CF2H, S(O)nR8, and S(O)2N(R9)R10; Y is chosen from CR11 and N; Z is chosen from O and NH; R3 is chosen from —C(O)R12 and —C(O)N(R9)R10; and n, R1, R2 and R4-R12 are defined herein; compositions comprising one or more such chemical entities; and methods of using one or more such chemical entities for modulating the activity of certain receptors (e.g., farnesoid X) or for the treatment or prevention of one or more symptoms of disease or disorder related to the activity of those receptors.
CN102860985A Tebipenem pivoxil oral preparation and preparation method thereof The invention relates to a tebipenem pivoxil-containing oral preparation and a preparation method of the tebipenem pivoxil-containing oral preparation. The preparation provided by the invention consists of tebipenem pivoxil and a pharmaceutic adjuvant as the active components. The pharmaceutic adjuvant contains beta-cyclodextrin. The tebipenem pivoxil oral preparation provided by the invention overcomes the defects that the grit feeling is produced when the tebipenem pivoxil oral preparation is taken, the patient compliance is poor and the preparation technology is complicate in the prior art, so that the tebipenem pivoxil oral preparation is an excellent preparation with good taste, high dissolvability, good stability and simple preparation technology.
WO2007138224A1 Nasal and buccal compositions for controlling snoring The invention relates to the use of a nasal composition and a buccal composition for preparing a combined composition to be used simultaneously, sequentially or separately for the treatment or prevention of snoring, especially for a person who snores heavily.
WO2014037480A1 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection The invention provides novel compounds having the general formula:, wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.
CA2660636A1 Nucleosides, drugs containing these and use thereof The invention relates to specific nucleosides and also to medicaments which comprise these nucleosides. The invention further relates to the use of such nucleosides for producing a medicament, more particularly for suppressing or reducing the development of resistance in cytostatic therapy.
EP1891064B1 N-amide derivatives of 8-azabicyclo[3.2.1]oct-3-yl as ccr1 antagonists The present invention relates to new antagonists of the interaction between the CCR1 Chemokine receptor and its ligands, including MIP-1α (CCL3), in particular new N-amide derivatives of 8-azabicyclo[3.2.1]oct-3-yl of formula (I).
WO2013084816A1 Agent for preventing and/or treating veisalgia [Problem] To provide an agent for preventing and/or treating veisalgia. [Solution] Provided is an agent for preventing and/or treating veisalgia, the agent including an ALA.
US7521478 Antitumor agents; synthetic derivatives equivalent to marine polyketide derived components isolated from bryozoan Myriapora truncata; removing protecting groups from intermediates Compounds of the general formula (I) or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof are provided: wherein the substituent groups defined by R are each independently selected from the group consisting of H, SiR′3, SOR′, SO2X, C(═O)R′, C(═O)OR′, C(═O)NR′, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aryl, heteroaryl or aralkyl; the group R′ is selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aminoalkyl, aryl, aralkyl and heterocyclic groups; and the group R″ is selected from the group consisting of H, OH, OR′, OCOR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, N(COR′)2, NHSO2R′, CN, halogen, C(═O)H, C(═O)R′, CO2H, CO2R′, CH2OR, substituted or unsubstituted alkyl, substituted or unsubstituted haloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkylidene, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; with the proviso that the compound is not compound 1, 3 or 4 of U.S. Pat. No. 5,514,708. The compounds have antitumour activity. A synthetic route is also provided.
US7569549 Crystallizing in water-miscible solvent, water, and mineral/organic acid Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A having the Formula I: wherein S is an organic solvent which is at least partially miscible with water, x is 1, 1.25, 1.5 or 2, y is 0, 0.5, or 1, the pseudopolymorph being characterized by the monoclinic space group P21 and average unit cell parameters comprising: crystal axis lengths of a=15.5-17.0 Å, b=15.5-17.0 Å, and c=17.5-19.5 Å, and angles between the crystal axes of α=γ=90° and β=106°-112°. In addition, this disclosure is directed to processes for the preparation of the substantially pure isostructural pseudopolymorphs of Formula I; to pharmaceutical compositions containing substantially pure isostructural pseudopolymorphs of Formula I; and to a method for the treatment of bacterial and protozoan infections, and inflammation-related diseases by administration of a pharmaceutical composition containing the substantially pure isostructural pseudopolymorphs of Formula I.
CN101897739A Hand anti-venom healing paste The invention discloses a method for preparing a hand anti-venom healing paste. The method is implemented by the following technical schemes of: firstly, freezing cerussa, verdigris, dried alum and minium at the temperature of -20 DEG C for 12 hours; taking the frozen materials out, and putting the frozen materials into a copper balm pan; striking a fire to decoct the materials for 40 to 60 minutes, and adding carbonized human hair ash during the decoction; and then decocting by using mild heating fire until the product is shaped into a ball and does not disperse when dropped into water. By using the hand anti-venom healing paste prepared by the method, the disease can be cured approximately in three days.
CN103417525A Application of zinc gluconate tablets and six vitamin pills in treating ametropic eyes The invention discloses application of zinc gluconate tablets and six vitamin pills in treating ametropic eyes. The application comprises the application of the zinc gluconate tablets and the six vitamin pills in treating hypermetropic eyes or hypermetropic amblyopic eyes with the diopters of +0.5D to +9.0D and presbyopic eyes with the diopters of +0.75D to +2.5D, the application of the zinc gluconate tablets, the six vitamin pills and adenosine disodium triphosphate injecta in treating primary myopic eyes with the diopters of -0.5D to -1.25D, and the application of the zinc gluconate tablets, the six vitamin pills, the adenosine disodium triphosphate injecta and phacolysin eye drops in treating the primary myopic eyes with the diopters of larger than -1.5D. According to the invention, the new application of multiple conventional drugs are realized, the zinc gluconate tablets, the six vitamin pills, the adenosine disodium triphosphate injecta and the phacolysin eye drops are adopted to treat ametropic eyes with different diopters and are effective in treatment.
US7019026 Modulators of Protein Tyrosine Phosphatases (PTPases) Disclosed are novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like, wherein n, m, X, Y, R1, R2, R3, R4, R5 and R6 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
WO2011110225A1 Adhesive patch for therapeutic agent delivery An adhesive patch for the delivery of at least one therapeutic agent, said patch comprising a soluble film incorporating said at least one therapeutic agent.
US7824713 Method for treating diaper rash using superhydrated bacteriostatic topical preparation with stable acid pH A method for treating diaper rash, leg ulcers and bed sores using super hydrated bacteriostatic topical preparation with a stable acid pH 5.82, by applying this topical application, which is a mixture of anhydrous lanolin (USP), water, boric acid powder (USP), edible corn starch, white petrolatum, cosmetic grade, and zinc oxide ointment (USP 20% zinc oxide) mixed in a paddle mixer at a temperature of about 100° F. to 107° F. then applying topically, the super hydrated bacteriostatic preparation, at room temperature, on the rash, leg ulcers, or bed sores.
US20050227995 Phenyl sulfoxides and phenyl sulfones The invention relates to phenyl sulfoxides and sulfones and processes for their preparation, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially Alzheimer's disease.
US7879547 Method of detecting the presence of asthma or allergies in a patient Several genes are upregulated in the lung of asthma or allergy sufferers. Many of the genes up-regulated in asthma are involved in arginine metabolism in the lung. Moreover, a set of 291 signature genes was found that can be used to indicate a patient's predilection for developing asthma or the patient's degree of suffering. Also, a set of 59 signature genes were found that indicate a patient's predilection for developing allergies. Many of the up-regulated genes relating to asthma were from the arginine metabolic pathway. Other genes, such as ADAM8, SPRR2A and SPRR2B were also strongly up-regulated in asthma. Treatment of asthma may be accomplished by administering compositions which decrease the levels of Arginase I, Arginase II, CAT2, or other arginase pathway members in the lung. Additionally, detection of altered levels of these proteins or the mRNA encoding them may be useful to diagnose the presence of asthma in a patient.
WO2009085277A3 Use of anti-connexin 43 polynucleotides for the treatment of abnormal or excessive scars Methods, compounds, compositions, kits and articles of manufacture comprising anti- connexin polynucleotides for prevention and/or treatment of abnormal scars, including keloid scars, hypertrophic scars, atrophic scars, and widespread scars.
US20100226911 Treating or preventing extracellular matrix build-up A method of treatment for treating, preventing, inhibiting or reducing extracellular matrix build-up in a body tissue or a bodily fluid transport vessel, in a subject, includes administering to a subject in need of such treatment an effective amount of a composition including a peptide agent including amino acid sequence LKKTET, a conservative variant thereof, or a peptide agent that stimulates production of an LKKTET peptide, or a conservative variant thereof, in the tissue.
US20110039920 Inhibitors of ikk-beta serine-theronine protein kinase Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5(carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl(25,4E)-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and tert-Butyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity.
US20110077301 Novel methods of administering a mixture of fatty acids for the treatment of non-human mammals Mixture of fatty acids, their derivatives, ester or methyl ester derivates thereof, which may be administered to non-human mammals by diffusion in to ambient air during at least seven consecutive days, with a rapid kinetic of diffusion during the first three days of administration.
EP1686991A1 Use of piketprofen for the preparation of a pharmaceutical composition to treat rosacea The invention relates to the use of picketprofen for the preparation of novel pharmaceutical compositions, more particularly dermatological compositions, which can be used to treat rosacea.
CN102525905A Tinidazole and sodium chloride injection and preparation method thereof The invention relates to a tinidazole and sodium chloride injection and a preparation method thereof. The injection is prepared from the following raw materials in percentage by weight/volume: 0.4 percent of tinidazole, 0.9 percent of sodium chloride, 0.005 to 0.5 percent of stabilizer, 0.01 to 0.05 percent of activated carbon, a proper amount of pH value regulator (the pH value is 3.5 to 5.5), and the balance of water for injection. The preparation method comprises the following steps of: putting the sodium chloride into a thick mixing tank, stirring the sodium chloride and water and dissolving to form a solution at the concentration of between 20 and 22 percent (g/ml), adding 50 percent of the activated carbon, stirring, boiling, cooling, performing pressure filtration, performing internal circulation for 10 minutes, and transferring into a thin mixing pot; putting the tinidazole into a container, adding water, stirring and dissolving, and transferring into the thin mixing pot; putting the stabilizer into the thin mixing pot, adding water, adding the residual activated carbon, adding water until the mixture reaches certain volume, stirring, refluxing for 15 minutes, and regulating the pH value to be 3.5 to 5.5 by using the pH value regulator; sampling, detecting the sodium chloride and the tinidazole, and cooling to 20 to 40 DEG C after the content of the sodium chloride and the tinidazole is qualified; and sequentially performing four-stage filtration and filling, sterilizing at the temperature of 121 DEG C, and warehousing after the product is proved to be qualified through light inspection. The problems that a tinidazole and sodium chloride injection is low in clarity qualification rate and is easy to crystallize in winter are solved.
US7405241 Administering nitrous oxide or xenon or donors thereof along with oxygen, nitrogen, and/or argon; stroke therapy; neuroprotectants A medicinal composition and method to treat or minimize post-ischemic brain cell deterioration that comprises nitrous oxide or a nitrous oxide donor and xenon or a xenon donor. The medicinal composition may be administered prior to or subsequent to a stroke.
US20120071550 Synergistic combinations of cartonoids and polyphenols The present invention provides a therapeutic composition comprising one or more polyphenols and one or more carotenoids selected from the group consisting of lutein, lycopene and beta-carotene. The invention also provides methods for inhibiting or reducing the production of superoxide ions, NO, TNF-alpha and/or PGE2 in a mammalian subject comprising administering to said subject the aforementioned therapeutic composition.
EP1042352B1 Androgenic steroid compounds and a method of making and using the same An androgenic steroid compound of formula (I) wherein: X, Y, Z, R?1, R2, R3, R5 and R6¿ are as defined herein.
WO2009070331A2 Compounds and methods for the selective inhibition of abcb1, abcc1 and abcg2 transporters and the treatment of cancers, especially drug resistant cancers and high throughput flow cytometry assay to detect selective inhibitors Compounds disclosed which inhibit ABCBl transporter protein are useful for treating diseases in which ABCBl transporter protein mediates the disease state, including numerous cancers, including hematopoietic cancers, including various leukemias, especially T-lineage acute lymphoblastic leukemia, as well as cancerous tumors, especially forms which exhibit multiple drug resistance. Pharmaceutical compositions which comprise an inhibitor of ABCBl transporter protein and at least one additional anticancer agent, optionally in combination with a pharmaceutically acceptable carrier, additive or excipient are another aspect of the present invention. A flow cytometry based, high-throughput screening (HST) assay that quantifies ABCBl efflux is also disclosed. Methods of identifying inhibitors of ABCBl, ABCG2 and ABCCl transporter proteins are also disclosed.
CN103462911A Preparation technique of freeze-dried powder injection The invention belongs to the technical field of medicinal preparations, and provides a preparation technique of a freeze-dried powder injection. The preparation technique comprises the following steps of cooling the prescription amount of 40%-90% of water for injection to 20-60 DEG C, regulating or not regulating pH, sequentially adding all prescription matters, stirring, measuring or regulating pH, supplementing water, adding active carbon of the prescription amount under the condition of temperature control, stirring and decoloring, filter pressing, filtering, and sterilizing, thereby obtaining a sterile liquid medicine; and separately bottling by penicillin bottles, carrying out freeze drying, and capping through rolling, thereby obtaining the freeze-dried powder injection. The preparation technique is simple to operate, has short production cycle, is applicable to industrial production, prevents products from decomposing due to high temperature, avoids slow compatibility of medicines, is accurate in measuring products, can produce products with a good appearance, is beneficial to improvement of the stability of medicines, and is convenient for long-term storage of medicines. The preparation technique is widely used for preparing freeze-dried powder injections of ligustrazine phosphate, sodium ozagrel, levocarnitine, and omeprazole and the like.
WO2010126967A1 Ex-vivo treatment of immunological disorders with pkc-theta inhibitors Disclosed is a method for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and atherosclerosis. Specifically, the invention relates to a method of treating an immunological disorder or atherosclerosis in a patient comprising treating blood from the patient, or a defined component of said blood, with an inhibitor of PKC-theta ex vivo and then re-administering the treated blood to the patient.
WO2011115513A9 A cytosine analogue, a method of preparation of a cytosine analogue, a dna methyltransferase 1 inhibitor, a method for dna methylation inhibition, the use of the analogue in the treatment of diseases associated with deviations from normal dna methylation This invention provides a cytosine analogue, a method of preparation of a cytosine analogue, a DNA rhethyltransferase 1 inhibitor, a method for DNA methylation inhibition, the use of the analogue in the treatment of diseases associated with deviations from normal DNA methylation. More precisely, the invention relates to various derivatives of cytosine, as well as methods of preparation of mono- and multi- 1,4,5 and 6-substituted cytosines. In general, the solution relates to providing effective modulators of DNA methylation which could be used in prevention and treatment of diseases associated with DNA methylation level disorders.
CN101903338A Phenyl acetic acid derivatives as inflammation modulators Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives of formula I wherein R1 is alkyl or cycloalkyl; R2 is halo, alky I, haloalkyl, alkoxy, haloalkoxy or cycloalkyl; and X is chloro or fluoro.
WO2008013248A1 Process for production of (±)-trans-4-(4- fluorophenyl)-3-hydroxymethylpiperidine A process for producing (±)-trans-4-(4-fluorophenyl)- 3-hydroxymethylpiperidine, comprising reducing (±)-trans-4-(4-fluorophenyl)-3-methoxycarbonylpiperidin-6 -one with a boron trifluoride-ether complex and sodium borohydride to produce a reaction solution, adding a mineral acid and a potassium salt to the reaction solution, adjusting the pH value of the solution to 0.5 to 4.0, removing any precipitate from the solution to produce a acidic solution, and then adjusting the pH value of the acidic solution to 11.0 to 12.5.
US20110166134 Glucosylceramide Synthase Inhibition For The Treatment Of Collapsing Glomerulopathy And Other Glomerular Disease A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.
WO2008058278A2 POLYMORPHS OF N2-(1, 1' - BIPHENYL - 4 - YLCARBONYL) - N1- [2- (4 - FLUOROPHENYL) -1, 1 - DIMETHYLETHYL]- L - α -GLUTAMINE Disclosed are novel polymorphic forms of N2-(1, 1'-biphenyl-4-ylcarbonyl)-N1-[2-(4- fluorophenyl)-1, 1-dimethylethyl]-L-α-glutamine, methods of preparing the polymorphic forms, compositions containing the polymorphic forms, and methods of treatment using the polymorphic forms.
WO2007098270A3 Co-crystals comprising vx-950 and pharmaceutical compositions comprising the same The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of salicylic acid, 4-amino salicylic acid, and oxalic acid. Also within the scope of this invention are methods of making and using the same.
CN103599107A Novel applications of bis(alpha-furancarboxylato)oxovanadium as anticancer medicine The invention relates to novel applications of bis(alpha-furancarboxylato)oxovanadium, a vanadium complex, as an anticancer medicine. Vanadium is a microelement essential for the human body. The bis(alpha-furancarboxylato)oxovanadium is an oxygen vanadium complex using alpha-furancarboxylic acid as a ligand, and is a potential anti-diabetic medicine, wherein the alpha-furancarboxylic acid is a metabolite of furfural in the human body. Researches discover that: the alpha-furancarboxylic acid has a strong cancer cell killing function; the IC50 of the alpha-furancarboxylic acid is smaller than the IC50 of cis-platinum or is equivalent to the IC50 of the cis-platinum; the alpha-furancarboxylic acid has stronger activity to cancer cells tolerant to the cis-platinum; alpha-furancarboxylic acid has smaller toxicity to normal human cells than the cis-platinum, and smaller acute toxicity to mice than the cis-platinum; and the alpha-furancarboxylic acid is high in water solubility and good in water solution stability, and therefore the bis(alpha-furancarboxylato)oxovanadium can be used as the anticancer medicine and used for treatment of malignancy.
CN101084988A Medicine for treating foot diseases and insole containing the said medicine The invention relates to a medicament for treating skin disease of foot and insoles containing the medicament, wherein the medicament is prepared from the following raw materials (by weight portions): flavescent sophora root 21-28%, ledebouriella root 21-28%, rhizome of Sichuan lovage 21-28%, dahurian angelica root 12-14%, talcum powder 12-14%. The insole includes a skin layer and a sandwich layer.
US20120101089 Anti-Emetic Substance The present invention provides a therapeutic solution for effective control of symptoms related to nausea and vomiting. The therapeutic solution is a pharmaceutical composition which combines anti-emetics of different classes. These classes include dopamine receptor antagonists, serotonin receptor antagonists, butyrphenones, and neurokinin receptor antagonists. The combination of different anti-emetics mitigates adverse affects of a single anti-emetic alone while increasing drug efficacy and decreasing cost of administration to the individual patient.
WO2008101202A1 N-17-alkylated prodrugs of opioids Compounds of formula (II) R1R2R3N+-(C(R1a)(R2a))-Ar-Z-C(O)-Y-(C(R1)(R2))n-N-(R3)(R4) A-II, in which R1R2R3N+, R1a, R2a, Ar, Z, Y, R1, R2, n, R3, R4 and A- have the meanings given in the specification, are useful as prodrugs for opioids (Example 13).
US7521417 Method and apparatus for preparing an acellular red blood cell substitute A process is disclosed for the preparation of an essentially tetramer-free, substantially stroma-free, polymerized, pyridoxylated hemoglobin. Also disclosed is an essentially tetramer-free, substantially stroma-free, polymerized, pyridoxylated hemoglobin product capable of being infused into human patients in an amount of up to about 5 liters.
CA2253287C A process for producing a recombinant polypeptide involving the addition of an inhibitor of metal-dependent proteases or chymotrypsins to the cell culture medium The present invention relates to a process for reducing the detrimental influence of certain proteases on recombinant human protein and polypeptide molecules, by adding an inhibitor of metal-dependent proteases or chymotrypsins to the cell culture medium. The invention also relates to a cell culture medium for cultivating cells expressing and secreting a biologically active recombinant human polypeptide containing an inhibitor of metal-dependent proteases or chymotrypsins, or a combination thereof. The invention further relates to use of recombinant factor VIII which has been produced in a cell culture medium according to the present process for the manufacture of a medicament for administration to a patient having the symptoms of hemophilia A. Also, the invention relates to a method for treatment of hemophilia A by administration of a therapeutically effective amount of recombinant factor VIII which has been produced in a cell culture medium according to the present process.
US20120238575 Antiproliferative pyrimidyl, fused pyrimidyl and pyrimidyl hydrazones The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.
CN201230969Y Coated creatine The utility model provides a coating creatine of which the active ingredients are creatines and (or) the compound particles thereof, and the surfaces of the creatines and (or) the compound particles thereof are coated by a coating of slowly-releasing coating material. The coating creatine can be slowly and constantly released in a human body so as to avoid the higher fluctuation of the creatines in the human body, to lead to the longer maintenance of the higher creatine concentration and to better support training and muscle growth; and besides, the surfaces of the creatines and (or) the compound particles thereof are coated by a layer of coating material, which is in favor of the release of the bitter and harsh taste of the creatine and the taking of the creatine.
US20060229308 Substituted pyrirmidin-4-ylamine analogues as vanilloid receptor ligands Substituted pyrimidyl-4-ylamine analogues are provided, of the Formula: (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate Vanilloid receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
US20110165257 Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea The present invention provides an oral pharmaceutical formulation comprising coated spheroids of a kinase inhibitor such as neratinib, which formulation is designed to reduce or eliminate side effects associated with existing oral formulations of kinase inhibitors.
US20080188478 Compounds Useful In Therapy Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents a group selected from H, CF3, and C1-6 alkyl (optionally substituted by C1-6 alkyloxy or triazolyl); R2 represents halo; Ring A represents a 5- or 6-membered heterocyclic ring containing at least one N atom (the ring being optionally bridged with two or more carbon atoms); R3 represents a 5- or 6-membered heterocyclic ring containing at least one atom selected from N, O or S, the heterocyclic ring being optionally substituted by one or more groups selected from C1-6 alkyl oxo or NH2, the heterocyclic ring being further optionally fused to a 5- or 6-membered aryl or heterocyclic ring containing at least one atom selected from N, O or S, the fused aryl or heterocyclic ring being substituted by one or more halo atoms; are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhea.
CN101723844A Agomelatine crystal form B, preparation method thereof and medicinal composition containing same The invention relates to an agomelatine crystal form B, a preparation method thereof and a medicinal composition containing the same.
WO2012119780A2 Novel lipids and novel phospholipids structures The invention relates to a lipids comprising or consisting of 1,3-diamidolipids or/and 1,2-diamidolipids or/and 2,3-diamidolipids or/and 1,3-diurealipids or/and 1,2-diurealipids or/and 2,3-diurealipids or/and 1,3 -dithiourealipids or/and 1,2-dithiourealipids or/and 2,3-dithiourealipids or/and 1,3-diacylurealipids or/and 1,2-diacylurealipids or/and 2,3-diacylurealipids or/and 1 -amidolipids or/and 1-urealipids or/and 1-thiourealipids or/and 1-acylurealipids or/and cyclic-amidolipids or/and cyclic urealipids or/and cyclic thiourealipids or/and cyclic acylurealipids, and their medical and non-medical use.
US20100190854 Composition and method to treat mastitis A method is provided to produce a treatment composition which is sprayed externally on to the udder of a cow to treat mastitis.
CN103613580A 3-hydroxyindole-2-ketone compounds for antitumor medicaments The invention relates to the field of medicinal chemistry, and specifically relates 3-hydroxy-3-[2,3-dihydroquinoline-4-keto-3-yl]indole-2-ketone compounds (I) and pharmaceutically acceptable salts thereof or pharmaceutically acceptable solvent mixtures thereof, a preparation method thereof, and uses of the compounds in preparing medicaments for preventing or treating diseases related to abnormal cell proliferation, morphologic change and the like, in particular medicaments for preventing or treating tumor growth and transfer.
CN101735151A Crystalline form I of lonidamine, preparation method thereof and composite containing the same The invention provides a crystalline form I of lonidamine, a preparation method thereof and a composite containing the same. Lonidamine crystal with the form I has the advantage of good leachability.
CN101139347B Banisterine derivative compound and uses thereof The present invention relates to a harmine derivative compound and the application. The compound is produced through the structural modification of the 1st, 2nd, 3rd, 7th and 9th pint of the parent nuclear of the beta-carboline of the harmine; thus the novel harmine derivative compound is synthesized with the enhanced anti-tumor activity and no toxicity of the nervous system. Through the screening research of the vitro and vivo anti-tumor model, the harmine derivative compound is found to have the significant anti-tumor activity (the tumor-inhibition rate of the tumor-bearing mice model reaches as high as 63.5 percent), have no neurotoxicity, and have the prospects of clinical application. The preparation method of the compound is simple; the collection rate is high; and the compound is used for the drugs of treating various tumor diseases.
CN101683348B Application of cholestane-3 beta, 5 alpha, 6 beta-triol in preparation of neuronal protection medicine The invention reveals that endogenous cholesterol metabolic product cholestane-3 beta, 5 alpha, 6 beta-triol (YC-5) has protection function for neuronal damage caused by cerebral ischemia, ischemia of spinal cord, epileptic seizure and convulsion and relates to an application of YC-5 in preparation of neuronal protection medicine. The YC-5 can be prepared from cholesterol through two steps. The primitive cell culture in vitro and spinal cord ischemia animal model proves that YC-5 has protection function for neuronal damage caused by cerebral ischemia, ischemia of spinal cord, epileptic seizure and convulsion. YC-5 in effective dose has no toxic and side reactions. YC-5 is an effective neural protectant which aims to multiple molecular mechanism and cures cerebral ischemia damage, spinal cord ischemia damage, epileptic seizure and convulsion.
CN103041372A Method for preparing thymalfasin composition for injection The invention discloses a method for preparing a thymalfasin composition for injection. The preparation method comprises the following steps: using thymalfasin, ganciclovir, mannitol and water for injection as raw materials; firstly, dissolving the mannitol into part of the water for injection to obtain a mannitol solution; adding and dissolving the thymalfasin and the ganciclovir into part of the water for injection to obtain a mixed solution of the thymalfasin and the ganciclovir; merging and uniformly mixing the mannitol solution with the mixed solution, then regulating the pH value of the mixed solution; adding the residual water for injection, adding medicinal carbon to fade, filtering, filling, and half packing; after half packing, putting the product in a freeze dryer for freezing and drying, and obtaining the product, namely the thymalfasin composition for injection; and finally packing and boxing the obtained product. The method combines the thymalfasin with the ganciclovir to prepare the thymalfasin composition drug used for inhibiting virus activation or curing viral diseases, and the thymalfasin composition drug has good drug stability. The thymalfasin composition can clinically better cure diseases.
CN1729994A Povidone iodine effervescence tablet for treating milk cow colpitis, its preparation process and application The invention provides a Povidone iodine effervescent tablet for preventing and treating cow's vaginitis, which is prepared from Povidone iodine, tartaric acid, sodium hydrogen carbonate, cross bonding polyvinylpyrrolidone, miropowdered silica gel, sodium dodecylsulfate, magnesium stearate, sodium chloride or lactose through dry method palletizing and pelleting.
US20100298758 Method for non-therapeutic or therapeutic photodynamic skin treatment In a method for non-therapeutic or therapeutic photodynamic treatment of a skin target area, a photosensitizer fluid incorporating a photosensitizing agent or a precursor for a photosensitizing agent is delivered to the target area, the photosensitizing agent having at least one absorption wavelength in a wavelength range higher than 400 nm. The target area is then exposed to light energy in a range of wavelengths comprising at least one absorption wavelength of the photosensitizing agent, the light energy being supplied to the target area in the form of at least one light pulse producing in the target area an accumulated energy density sufficient for photodynamic activation of the photosensitizing agent. The photosensitizing agent or precursor is incorporated in the photosensitizer fluid with a concentration in the range from 0.1 to 2.0% preferably from 0.1 to 0.9%, and the photosensitizer fluid is delivered to the target area in the form of a number of repeated spray doses during an overall delivery time ranging from 0.25 to 8 hours. The method can be applied to cosmetic treatments for skin rejuvenation, reduction of wrinkles, treatment of telangiectasia or removal of hair as wells a medical treatment of dermatologic diseases such as acne vulgaris, acne scars, rosacea, psorieasis, actinic keratoses, basal cell carcinoma, Bowen's disease or eczema.
US6994283 Method for pulverizing to fine powder The present invention has for its object to provide a method of micronizing (E)-4-[2-[2-[N-acetyl-N-(4 -methoxybenzenesulfonyl)amino]phenylethenyl]pyridine 1-oxide while maintaining its crystalline. The present invention relates to a method of micronizing the above compound characterized in that the compound is comminuted, for example, to the extent that the mean particle diameter of the compound will be 1˜25 μm with 50 μm and larger particles accounting for 2% or less with a mill of the open-circuit pulverizing type.
WO2008028314A1 Catechol derivatives, composition and application thereof Disclosed are compounds of formula (I), which can be used for preparation of pharmaceutical composition preventing and treating diabetes or ischemic diseases and complications thereof. ( I )
CA2356157C Combinations of cholesteryl ester transfer protein inhibitors and fibric acid derivatives for cardiovascular indications The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include a fibric acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.
CN102618547A Nucleic acid aptamer rich in guanine The invention discloses a nucleic acid aptamer rich in guanine and application thereof. The nucleic acid aptamer is at least one of the following nucleic acid aptamers (1) to (4): (1) DNA (Deoxyribonucleic Acid) molecule shown as SEQ ID NO: 1; (2) DNA molecule shown as SEQ ID NO: 2; (3) DNA molecule shown as SEQ ID NO: 3; and (4) DNA molecule shown as SEQ ID NO: 4. The invention provides a nucleic acid aptamer medicament for treatment of cancer. Compared with other tumor chemotherapy medicaments, the nucleic acid aptamer medicament has many advantages of suppressing specificity of tumor cell proliferation, easiness in synthesis and modification, no immunogenicity, capability of quickly penetrating tissues and good pharmacokinetics.
CN103073562A Method for refining cefamandole nafate, cefamandole nafate and application thereof The invention provides a method for refining cefamandole nafate, which comprises the following steps: (1) mixing lower alcohol and acetone or mixing lower alcohol and ethyl acetate to obtain a mixed solvent, wherein the volume ratio of the lower alcohol to the acetone or that of the lower alcohol to the ethyl acetate is (1-2) : (5-10); (2) dissolving the crude cefamandole nafate in a stirring manner into water for injection, and adjusting pH to 6-8 to obtain a crude solution; (3) when stirring, dropwise adding the mixed solvent into the crude solution, and then, dropwise adding ethyl acetate or acetone with the volume 30-40% of that of the mixed solvent, so as to obtain a suspension; and (4) cooling the suspension to 3-5 DEG C, standing for devitrification for 12-36 hours, vacuum filtration and drying to obtain refined cefamandole nafate. The invention further provides cefamandole nafate produced according to the refined method, sterile composition powder-injection preparation containing the cefamandole nafate, and application of the cefamandole nafate in preparing antibacterial agents.
WO2008106635A1 Pyrimidine-2,4-diamine derivatives and their use as jak2 kinase inhibitors Pyrimidine-2,4-diamines derivatives having activity as JAK2 kinase inhibitors are disclosed, as well as pharmaceutical compositions and methods for using the same in the treatment of cancer and other JAK2 kinase-associated conditions.
CA2706381A1 Processes for preparing a substituted gamma-amino acid The present invention is related to processes suitable for industrial synthesis of pregabalin from (i?)-(-)-3-(carbamoylmethyl) -5-methylhexanoic using sodium hypochlorite as described herein. In addition, the present invention is related to pregabalin which is substantially free of impurities and pharmaceutical compositions comprising pregabalin.
US7169810 Phenylalkyleneoxybenzene derivatives; insulin resistance; diabetes, obesity, dyslipidemia treatment; hypotensive agents The present invention releates to certain novel guanidine or amidine acid derivatives and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.
US7307069 Inflammatory diseases and cancers; promotion of apoptosis; may have phosphorothioate, 2'-O-(2-methoxyethyl) sugar, and/or 5-methyl cytosine modifications; useful prophylactically, and as clinical research and diagnostic tools. Compounds, compositions and methods are provided for inhibiting the expression of human STAT3. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding STAT3. Methods of using these oligonucleotides for inhibition of STAT3 expression and for promotion of apoptosis are provided. Methods for treatment of diseases, particularly inflammatory diseases and cancers, associated with overexpression or constitutive activation of STAT3 or insufficient apoptosis are also provided.
CN102060792A 2'-aminochalcone-zole compounds, pyrazoline and cyclopropyl azole derivatives thereof and preparation method and applications of compounds The invention relates to 2'-aminochalcone-zole compounds with structures shown in general formulas (I, II, III, IV and XIII) and pharmaceutically acceptable salts thereof, wherein amine groups are introduced onto chalcone skeletons while the zole-ring displacement of alpha-site can be realized; and the invention also relates to 2'-aminochalcone-zole compound-based pyrazoline derivatives with structures shown in the general formulas (V, VI, VII, VIII, XIV and XV) and pharmaceutically acceptable salts thereof, and relates to 2'-aminochalcone-zole compound-based cyclopropyl zole derivatives with structures shown in general formulas (IX, X, XI, XII, XVI and XVII) and pharmaceutically acceptable salts thereof. The invention relates to the antimicrobial activities and antitumor activities of the 2'-aminochalcone-zole compounds, the pyrazoline derivatives and cyclopropyl zole derivatives and the pharmaceutically acceptable salts. The invention also relates to medical applications of the compounds.
CN103381268A Solid pharmaceutical composition including proton pump inhibitor The invention relates to a solid pharmaceutical composition including a proton pump inhibitor and provides the solid pharmaceutical composition including the proton pump inhibitor and a preparation method thereof. According to the invention, active components and at least one non-active component are ground so as to reduce a particle size, which enables a drug release speed and drug bioavailability to be improved.
US7560454 1-(4-(10,11-dihydro-5H-pyrrolo[2,1-c](1,4)benzodiazepine-10-ylcarbonyl)-2-methyl-benzylcarbamoyl)-4methoxy-L-proline-N,N-dimethylamide; vasopressin agonists particularly useful in the treatment of urogenital disorders central diabetes insipidus, nocturnal enuresis and nocturia; blood disorders This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.
CN101468000B Application of bulleyaconitine A in preparing medicament for treating primary erythermalgia The invention relates to an application of bulleyaconitine A to preparing a medicament treating primary erythromelalgia, and belongs to a medicament containing effective organic components, especially to a medicament using bulleyaconitine A to treat diseases. The medicament comprises excipient having filling, binding, disintegrating and lubricating functions, which is mixed with the bulleyaconitine A and then pressed into tablets. Each bulleyaconitine A tablet contains 0.1-0.7mg of bulleyaconitine A or 0.2-0.4mg of bulleyaconitine A. Experiments show the bulleyaconitine A is necessary to treat primary erythromelalgia. Pharmacological mechanisms show that bulleyaconitine A increases sodium current of wild NaV1.7 cell strains by means of concentration dependence so as to cause an activatingcurve to move to hyperpolarizing direction and inhibiting effect thereof on activated Na<+> current can reach 90%.
CN102958928A Dimeric SMAC Mimetics The invention provides small molecule mimics of the Smac peptide that are dimers or dimer-like compounds having two binding domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
US20120016031 Biphenyl compound selective agonists of gamma rar receptors Biphenyl compounds having the formula (I): are useful for preventing/treating pathologies linked to a deficiency of the activation of the RAR gamma receptor, e.g., for treating a pathology linked to a cell differentiation and/or proliferation disorder, for treating acne, for treating psoriasis.
CN101822736A Novel biological bactericide and preparation method thereof The invention relates to a novel biological bactericide, which comprises the following components by volume ratio: 0.01-10% of grapefruit seed extract, 0.02-10% of epsilon-polylysine, citric acid and deionized water. The preparation method of the biological bactericide comprises the following steps: by volume ratio, A, selecting 0.01-10% of grapefruit seed extract and 0.02-10% of epsilon-polylysine; B, fully mixing the two components in a mixing tank to obtain an original biological bactericide liquid; C, adding the citric acid in the original biological bactericide liquid obtained from the step B, so that the ph value is 6.8-7.2; and D, adding the deionized water in the liquid obtained from the step C so as to finally obtain the biological bactericide. Compared with the prior art, the technical scheme of the invention has the beneficial effects that: the invention technology uses pure biological sources, and the biological bactericide is colorless and tasteless, has no restricted use areas, can enter the mouth, the nose, eyes and other parts, and has no toxicity and does not produce drug resistance.
EP0871485B1 COMPOSITIONS AND METHODS FOR CATALYZING HYDROLYSIS OF HIV gp120 A catalytic antibody and components thereof which cleave HIV gp120 are disclosed. Methods of isolating, cloning and purifying such antibodies or antibody components from patients are also described. The compositions described may provide utility in the treatment of HIV infection.
WO2014140695A1 Solid oral formulation of a pyrrolidine substituted flavone compound The present invention relates to a pharmaceutical composition providing a self emulsifying drug delivery system (SEDDS) for oral administration, comprising a compound, (+) trans-2-(2-chloro-phenyl)-5,7-dihydroxy-8-(2-hydroxymethyl-1- methyl-pyrrolidin-3-yl)-chromen-4-one or a pharmaceutically acceptable salt thereof, along with one or more surfactant and a solubilizer. The present invention also relates to a process for preparation of said pharmaceutical composition and use of the pharmaceutical composition in the treatment of a disease or disorder selected from cancer, polycystic kidney disease, nephrological disorder, psoriasis, immunological disorder involving unwanted proliferation of leukocytes, restenosis, proliferative smooth muscle disorder, radiation induced mucositis, viral infection, mycotic infection or cardiovascular abnormality.
WO2011017905A1 Use of senkyunolide i in manufacture of medicament for anti-depression, treating migraine and other diseases related to serotonergic system The present invention provides the use of senkyunolide I in the manufacture of the medicament for anti-depression, treating migraine and other diseases related to serotonergic system
CA2780205A1 Methods of treating elevations in mtor signaling Subjects having elevated signaling of a mammalian target of rapamycin (mTOR) are treated with compositions that include at least one compound that activates a Group 1 mGluR. In an embodiment, the subject has tuberous sclerosis complex (TSC). In an embodiment, the compound is a Group 1 mGluR agonist. In another embodiment, the compound is a Group 1 mGluR positive allosteric modulator.
US20100216806 Ortho aminoamides for the treatment of cancer Compounds of formula are HDAC inhibitors. These compounds are useful for the treatment of diseases such as cancer in humans or animals.
CN1771984A New use of extracellular polysaccharide of halophilous aphanothece The present invention discloses the new use of extracellular polysaccharide of halophilous aphanothece. The research of the present inventor shows that extracellular polysaccharide of halophilous aphanothece has the effect of regulating bodyí»s immunity and may be prepared into immunoregulating medicine. The animal experiments show that extracellular polysaccharide of halophilous aphanothece may be also prepared into antitumor medicine and pneumonia preventing and/or treating medicine, with the effective dosage being 6-8 mg/kg body weight every day. The present invention has great clinical value and economic value.
US20110053981 Methods and Compositions Using Cholinesterase Inhibitors The invention provides methods for treating and/or preventing Alzheimer's disease, psychiatric illnesses, encephalitis, meningitis, fetal alcohol syndrome, Karsakoff's syndrome, anoxic brain injury, cardiopulmonary resuscitation injuries, diabetes, Sjogren's syndrome, mental retardation, developmental delay, menopause, strokes, macular degeneration, neuronal loss associated with macular degeneration, sleep disorders, severe Alzheimer's disease, jet lag, post-traumatic stress disorder, anxiety disorders, panic attacks, obsessive-compulsive disorder, amnesia, and other disorders by administering to a patient in need thereof at least one cholinesterase inhibitor. The invention also provides novel pharmaceutical compositions that can be administered to the eyes or to the nose of patients. In one embodiment, the cholinesterase inhibitor is donepezil, a stereoisomer thereof and/or a pharmaceutically acceptable salt thereof. In other embodiments, the cholinesterase inhibitor can be one or more of phenserine, tolserine, phenethylnorcymserine, ganstigmine, epastigmine, tacrine, physostigmine, pyridostigmine, neostigmine, rivastigmine, galantamine, citicoline, velnacrine, huperzine, metrifonate, heptastigmine, edrophonium, TAK-147, T-82, and upreazine.
CN102920687A Application of 1-(3,4,5-trihydroxy) phenyl-1-dinone in preparation of medicament for preventing or treating melanoma The invention discloses application of 1-(3,4,5-trihydroxy) phenyl-1-dinone in preparation of a medicament for preventing or treating melanoma, and relates to an organic small molecular compound. 1-(3,4,5-trihydroxy) phenyl-1-dinone can be used as a medicinal composition of a medicinal carrier or an excipient or an additive, and the medicinal composition has the effect of preventing and treating the melanoma. Various medicinal excipients, additives or carriers can be added in the medicinal composition for treating the melanoma. The medicament and the medicinal composition can be prepared into other dosage forms of enteric or non-enteric administration such as tablets, capsules, granules and injection according to the known methods in the field. The application range of 1-(3,4,5-trihydroxy) phenyl-1-dinone in disease treatment is expanded.
US20110053862 Compositions comprising survivin sirna and methods of use thereof The present invention provides siRNA nucleic acid molecules that inhibit survivin expression. Methods of using the nucleic acid molecules are also provided.
US20080090843 Pharmaceutical formulation for treatment of HBV infection comprising a compound that inhibits the activity of a Src kinase in an amount effective to inhibit HBV replication and a pharmaceutically acceptable carrier The present invention relates to therapeutic protocols and pharmaceutical compositions designed to target HBx mediated activation of Src kinase, members of the Src 5 tyrosine kinase family and components of the Src kinase family signal transduction pathways for the treatment of HBV infection and related disorders and diseases, such as HCC. The invention further relates to pharmaceutical compositions for the treatment of HBV infection targeted to HBx and its essential activities required to sustain HBV replication. The invention is based, in part, on the Applicants' discovery that activation of Src kinase signaling cascades play a fundamental role in mammalian hepadnavirus replication. Applicants have demonstrated that HBx mediates activation of the Src family of kinases and that this activation is a critical function provided by HBx for mammalian hepadnavirus replication.
WO2014000719A1 Novel pharmaceutical solid forms of (1s,2s,3r,5s)-3-[7-[(1r,2s)-2-(3,4difluorophenyl)cyclopropylamino]-5-(propylthio)-3h-[1,2,3]triazolo[4,5-d]pyrimidin-3yl]-5-(2-hydroxyethoxy)cyclopentane-l,2-diol Solid state structures of (1S,2S,3R,5S)-3-[7-[1R,2S)-2-(3,4-Difluorophenyl)cyclopropylamino]-5- (propylthio)-3H-[1,23]triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol (hereafter referred to as Ticagrelor) in the form of a stable 3-hydroxy-2-naphthoic acid co-crystal solid form as well as a 1,4-dioxane solvate, and processes for the preparation thereof.
CN101229222A Liquorice extractive for decreasing medicine heart toxicity and applications thereof The invention provides a liquorice extract for alleviating the toxicity of heart medicines; the extract originats from legume liquorice, such as the dried roots and rhizomes of Glycyrrhiza uralensis Fisch, G. Inflata Bat, and G Glabra L. The main active components are triterpenoid saponin and materials of flavonoids glycosides; wherein, the content of triterpenoid saponin is 10 to 30 percent, and the content of flavonoids is 20 to 40 percent. The in-vivo and in-vitro experiments prove that the liquorice extract has significant protection effect for heart injury induced by adriamycin, at the same time, the liquorice extract does not lower the antitumor effect for anthracycline antitumor medicine; the extract can prevent and lighten the toxicity of anthracycline heart medicines, so the extract improves the efficacy and enlarges the clinical application range; the extract can also be applied in the preparation of anthracycline antitumor medicines for treating heart toxicity.
US20090082422 Deuterium-enriched levetiracetam The present application describes deuterium-enriched levetiracetam, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2011107248A1 NOVEL COMPOUNDS FOR MODULATION OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ GAMMA, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASE The invention provides modulators for the orphan nuclear receptor RORγ and methods for treating RORγ mediated diseases by administrating these novel RORγ modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
CN101812059A Nitric oxide donor-type farnesyl thiosalicylic acid derivative, and preparation method and medical application thereof The invention discloses a nitric oxide (NO) donor-type farnesyl thiosalicylic acid (FTA) derivative, and pharmaceutically acceptable salt, a preparation method and medical application thereof. The FTA derivative is a compound obtained by carrying out heterozygosis on a NO donor furazan nitrogen oxide and Ras protein inhibitor FTA by an ester bond or an amido bond. Pharmacological test results show that the FTA derivative can reserve the Ras protein inhibiting activity of FTA and simultaneously releases high-concertration NO to induce cancer cell apoptosis and enhance the inhibiting action on cancer cell proliferation; compared with the FTA, the FTA derivative has more excellent anti-tumor activity, and therefore, the compound can be suitable for treating various clinical malignant tumours.
CN101744812A Liniment for treating impetigo The invention discloses a liniment for treating impetigo, aiming to provide a pharmaceutical composition for being directly used on the wound so that the impetigo can be quickly treated. The liniment is prepared from the following raw materials: a medicine having a chemical name that is D-threo-(-)-N-[alpha-(hydroxy methyl)-beta-hydroxyl-p-nitrophenyl ethyl]-2,2-dichloroacetamide; a medicine having a chemical name that is 1'S,6'R)-6'-methyl-2', 4,6-trimethoxyl-7-chlorine-spiro[benzofuran-2(3H), 1'-[2] vinyl cyclones-3, 4'-diketone; predisone tablet; and chlorpheniramine maleate tablet. The four medicines are mixed according to the weight ratio of 1: 2: 2: 2 to prepare a suspension liniment. When in use, the liniment for treating impetigo has the advantages of quick drug effect, wide application range, quick treatment and no recrudescence.
CA2857487A1 Insulin-mimetics as therapeutic adjuncts for bone regeneration Methods of promoting bone healing or regeneration by locally administering insulin mimetic agents to patients in need thereof and new uses of insulin-mimetic compounds for accelerating bone-healing processes are disclosed. Bone injury treatment and void filler devices, products and kit suitable for local administration of insulin-mimetic agents or compositions thereof to patients in need of such treatment are also disclosed.
US7754750 a -5 substituted 1-H,3-H-imidazolidine-2,4-dione such as 5-(2-{[4-(4'-fluoro[1,1'-biphenyl]-4-yl)-1-piperazinyl]sulfonyl}ethyl)-2,4-imidazolidinedione; protease inhibitors, especially metalloelastase (MMP12) Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
CN1582954A Composition of roxithromycin and ambroxol A composite medicine for treating bronchitis, bronchopneumonia, pneumonia, asthma, nasosinusitis, tympanitis, etc is prepared from roxithromycin and ambroxol in weight ratio of (1-3):(0.3-0.6).
CN103230387A Entero-soluble type compound acidifier pellet and preparation method thereof The invention discloses an entero-soluble type compound acidifier pellet and a preparation method thereof, which can be used for solving the problems that the existing acidifier is unobvious in effect, capable of causing stimulation to gastric mucosa due to high release speed in the stomach, capable of affecting gastric acid secretion of piglets. The entero-soluble type compound acidifier pellet comprises the following components in percentage by weight: 75%-90% of pellet core and 10%-25% of enteric coating layer, wherein the pellet core includes 40%-60% of compound organic acid and 40%-60% of auxiliary materials. The invention further provides a preparation method of the entero-soluble type compound acidifier pellet. The pellet disclosed by the invention is enabled to be insoluble in the stomach, soluble in small intestines and large intestines, so that medicine liquor is released in a located manner, and therefore, the effect of adjusting acid-base equilibrium of intestinal tracts of weaned pigs and gastrointestinal tract growth and development can be improved. Moreover, the entero-soluble type compound acidifier pellet is easily available in material, reasonable in composition, low in production cost, simple in process flow and easy to popularize and use.
CN101066964A Juglone possessing anti cancer activity and its prepn The present invention discloses one kind of juglone possessing anticancer activity and its preparation process. The new juglone compound is extracted and separated from green walnut peel or walnut branch and leaf. It is diaryl heptane compounds with molecular formula of C21H24O5 and C20H22O3. Pharmacological experiment shows the new juglone has high anticancer activity and is hopeful in being developed into new anticancer medicine.
US8673280 Pharmaceutical composition for intracellar acidification with cis-urocanic acid A pharmaceutically acceptable agent able to acidify the cell cytoplasm for the manufacture of a pharmaceutical composition useful for causing immunosuppression in a person or animal, where an effective amount of the agent is administered in an essentially non-dissociated form to the person or animal, and where the agent is admixed with a carrier to adjust the pH of the composition to the pH range 6.1 to 7.0. A pharmaceutical composition is also disclosed.
US20090123516 Drug delivery from implants using self-assembled monolayers-therapeutic sams Disclosed are medical devices comprising one or more surfaces, one or more SAM molecules attached to the one or more surfaces of the medical device, and one or more therapeutic agents attached to the one or more self-assembled monolayer molecules. Also disclosed are medical devices comprising one or more surfaces, one or more self-assembled monolayer molecules attached to the one or more surfaces of the medical device, one or more linkers comprising a first functional group and a second functional group, the first functional group attached to the self-assembled monolayer molecule and a therapeutic agent attached to the second functional group. The therapeutic agent may be attached to the SAM molecule via a linker. The present invention also concerns methods of administering a therapeutic agent to a subject, comprising contacting the subject with one of the medical devices set forth herein.
US7176327 Water soluble, biologically inert Pt(IV) compounds which can be converted to cytotoxic Pt(II) species by photoactivation; reduced side effect anticancer drugs The present invention provides a compound of formula (I): PtIV(N3)2X1X2Y1Y2, wherein X1 and X2 are the same or different and each one is a group NR1R2R3 wherein R1, R2 and R3 are the same or different and each can be any one of H and optionally substituted alkyl, aryl, aralkyl, acyl, cycloalkyl, heterocyclyl, alkenyl, aralkenyl, alkinyl, cycloalkenyl, or X1 and X2 together represent a group R1R2NR4NR1R2 wherein R1 and R2 have the same meaning as before, and R4 represents an optionally substituted divalent, saturated or unsaturated, alkyl chain, an optionally substituted divalent, saturated or unsaturated cycloalkyl or an optionally substituted divalent aryl, or R4 or two or more of R1, R2, R3 and R4 and the respective N atom(s) to which they are linked, represent an optionally substituted heterocyclyl having at least one ring containing said N atom(s); and Y1 and Y2 are the same or different or when cis together represent a divalent moiety Y3, wherein at least one of Y1 and Y2, or Y3, is a substantially labile ligand in the analogous Pt(II) complex without the azide groups, while being substantially resistant, in vivo, to hydrolysis and physiological reducing agents. One or more of R1, R2, R3 and R4, may further represent a covalently bonded link to at least one further complex of formula (I) to form a dimer or oligomer, or to a targeting moiety having affinity for a predetermined tissue or cell type.
WO2008059238A1 Benzenesulfonamide compounds as edg-1 antagonists useful in the treatment of cancer This invention relates to novel compounds of formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds possess Edg-1 antagonistic activity and are accordingly useful in the treatment and/or prophylaxis of cancer.
US20090092543 Methods of treating and preventing inflammatory bowel disease involving il-13 and nkt cells The present invention provides a method of treating or preventing the inflammatory response of ulcerative colitis or Crohn's disease in a subject comprising administering to the subject an effective amount of a substance that inhibits the binding of IL-13 to IL-13 receptors on NKT cells or delivers an effector molecule to the NKT cells.
WO2009013166A1 3-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-1-propanone and use thereof as an antimicrobial active ingredient Antimicrobially active 3-(4-hydroxy-3-methoxyphenyl)-1 -(4-hydroxyphenyl)-1 - propanone of the following formula 1 is described, as is a method for producing this compound and the use thereof as an antimicrobial active ingredient. Formula (I).
CN101081209A Anticancer composition containing tyrosine kinase restraining agent and taxane The slow released anticancer injection containing tyrosine kinase inhibitor and/or taxane consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer components of tyrosine kinase inhibitor and/or taxane and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The suspending agent is carboxymethyl cellulose, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow releasing supplementary material is selected from p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP/TC), etc. The anticancer composition may be also prepared into slow released implant, and the released injection and slow released implant may be injected or set in tumor for slow releasing to maintain effective medicine concentration for over 40 days, and has obviously lowered systemic reaction on the medicine and capacity of enhancing the chemotherapeutic and radiotherapeutic effect.
US7744903 Epitopes confirmed to be recognized by T-cells derived from herpetic lesions or uterine cervix; vaccination; host cells The invention provides HSV antigens that are useful for the prevention and treatment of HSV infection. Disclosed herein are antigens and/or their constituent epitopes confirmed to be recognized by T-cells derived from herpetic lesions or from uterine cervix. T-cells having specificity for antigens of the invention have demonstrated cytotoxic activity against cells loaded with virally-encoded peptide epitopes, and in many cases, against cells infected with HSV. The identification of immunogenic antigens responsible for T-cell specificity provides improved anti-viral therapeutic and prophylactic strategies. Compositions containing antigens or polynucleotides encoding antigens of the invention provide effectively targeted vaccines for prevention and treatment of HSV infection.
CN102993186A Novel piperazine derivative The invention discloses a novel piperazine derivative with a structure as formula 1, wherein R is a carbamido or thioureido un-substituted or substituted by a substituent group, and the substituent group is selected from C1-C8 alkyl, C2-C6 alkenyl, C3-C6 naphthenic base, nitryl, hydroxyl, methylol, phenyl or substituted phenyl. The invention further describes a method for preparing the piperazine derivative. The invention further relates to the activity of the compound to the central nervous system.
US20090312374 Derivatives of 4,6-disubstituted 1,2,4-triazolo- 1,3,4-thiadiazole, a process and uses thereof The present invention is in relation to the derivatives of 4,6-disubstituted 1,2,4-triazolo-1,3,4-thiadiazole and a process to synthesize the said derivatives. Also, the present invention was able to establish the activity of the instant derivatives against anti-cancerous activity specific to cervical and oral cancer.
EP1655023A1 Botulinum toxin implat A biocompatible implant for continuous in vivo release of a neurotoxin over a treatment period extending from one month to five years. The implant can be made of casting a solution,of a polymer, such as an ethyl vinyl acetate copolymer and the neurotoxin. The neurotoxin can be a botulinum toxin.
EP1542528B1 A method of treatment and prophylaxis The present invention relates generally to a method for treating or preventing or otherwise ameliorating the effects of inflammatory conditions such as but not limited to chronic immune-mediated inflammatory diseases. The present invention further provides pharmaceutical compositions comprising agents which inhibit one or more inflammatory cytokines and/or which down-regulate expression of genes which encode inflammatory cytokines. Such compositions are useful in the treatment and prophylaxis of inflammatory conditions such as inflammatory arthritis amongst other chronic immune-mediated inflammatory diseases. The present invention further provides an animal model for studying the kinetics of and/or screening for agents useful in the treatment or prophylaxis of inflammatory conditions.
US20120093878 Pharmaceutical compositions containing a biguanide and a thiazolidinedione The present invention relates to pharmaceutical compositions that include a combination of a biguanide present in an extended-release form and a thiazolidinedione present in an immediate-release form. The present invention further relates to the processes for preparing such compositions.
US20080032918 Gene expression or biosynthesis inhibition by locally administering inhibitors of angiotensin-converting enzyme, angiotensin type 1 receptors, or sodium-hydrogen exchange type-1 proteins; antiinflammatory agents, myocardial antiischemic agents, anaphylaxis; sustained release implants, stents, inhalers The invention relates to the discovery that renin is present in mast cells and can act in a localized manner to initiate and/or exacerbate a number of conditions. Thus, the invention provides methods for treating cardiac, vascular, lung, liver, cervical, intestinal, muscle, pancreatic, brain, kidney, skin and other conditions that involve inhibiting the synthesis and/or release of renin from mast cells and/or inhibiting the activity of renin after release from mast cells. The methods of the invention can also involve inhibiting elements of the local renin-angiotensin system (e.g. inhibiting ACE and angiotensin II receptors), thereby inhibiting angiotensin II produced locally from mast-cell-derived renin.
CN1883498A Compound puerarin for treating cardiovascular and cerebrovascular disease The present invention relates to a medical composition comprising biological flavone or its derivatives and gynostemma pentaphyllum for preventing and curing cardiovascular disease and cerebrovascular disease, in particular heartstroke, myocardial infarct, coronary heart disease, cerebral thrombosis or cardio-cerebral tissue ischemia. The present invention also relates to medical preparation including the medical composition, its preparation and application of biological flavone or its derivatives and gynostemma pentaphyllum in preparing medicines for curing cardiovascular disease and cerebrovascular disease. The present medicine has virtues of high biological utility ratio, small poisonous side effect and small dosage etc. and is suitable for forming into various solid and liquid preparations.
US6916837 Such as 2-(6-amidino-2-naphthyloxy)-5-methanesulfonyl-aminobenzoic acid trifluoroacetate; blood coaggulation factor VII inhibitors Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 aryl, etc. and R2 represents hydrogen atom, etc.), etc., Ar1 represents 2,6-naphthylene, etc., R3 represents hydrogen atom, etc. and Y represents carboxyphenyl, etc.} and their pharmacologically acceptable salts or solvates.
WO2006090935A1 Acerola fruit-derived pectin and use thereof Discloses is an acerola fruit-derived pectin in the form of a complex with aceronidin that is a novel polyphenolic compound or a hydrolysate of the pectin. The pectin can be used as an antioxidative agent or the active ingredient for a skin-whitening agent.
CN101606931B Erdosteine composition and preparation method thereof The invention provides an Erdosteine composition which consists of the following components by weight portions: 130 to 170 portions of Erdosteine, 35 to 65 portions of lactose, 30 to 70 portions of microcrystalline cellulose, 20 to 40 portions of low substituted hydroxypropyl cellulose, 1 to 5 portions of acesulfame, 10 to 30 portions of sodium carboxymethyl starch and 0.1 to 0.5 portions of magnesium stearate; the invention also provides a preparation method of the Erdosteine composition, comprising the following steps of: preparing materials and pelleting; mixing the Erdosteine and the low substituted hydroxypropyl cellulose evenly, then grinding, adding the sodium carboxymethyl starch, adding absolute ethyl alcohol, wet-mixing, cutting, drying, granulation and tabletting; mixing granules and microcrystalline cellulose evenly, adding the lactose, the acesulfame and the magnesium stearate for pelleting, subpackaging and obtaining the Erdosteine composition. The Erdosteine compositionhas good dispersible uniformity and high drug dissolution efficiency.
EP1694317A1 Copper antagonist compounds Copper antagonist compounds and the use of such compounds in methods for the treatment, prevention, or amelioration of various disorders that would be benefited by reduction in copper, for example copper (II), including neurodegenerative and other disorders.
WO2012014746A1 Α-lipoic acid complex Provided are an α-lipoic acid complex obtained by complexing R-α-lipoic acid or S-α-lipoic acid, R-dihdyro-α-lipoic acid or S-dihdyro-α-lipoic acid, or an alkali metal salt or an alkaline earth metal salt thereof, and a method for producing the α-lipoic acid complex. An α-lipoic acid complex, which is stable to heat and an artificial gastric acid solution and has a high purity, can be produced by, for example, adding cyclodextrin to an aqueous solution containing, dissolved therein, R-α-lipoic acid or S-α-lipoic acid, R-dihdyro-α-lipoic acid or S-dihdyro-α-lipoic acid, or an alkali metal salt or an alkaline earth metal salt thereof and thus complexing R-α-lipoic acid or S-α-lipoic acid, R-dihdyro-α-lipoic acid or S-dihdyro-α-lipoic acid, or the alkali metal salt or the alkaline earth metal salt thereof at a high probability.
WO2011034051A1 Novel cyclic squaramide derivatives Compounds represented by general formula (1) or salts thereof. In general formula (1), A is an aromatic hydrocarbon ring or an aromatic heterocycle (with the ring and the heterocycle being optionally substituted); R1 to R11 may be the same or different and are each a hydrogen atom, a halogen atom, hydroxyl, mercapto, amino, or the like; R1 and R2 may be united to form a hydrocarbon ring or a heterocycle (with the ring and the heterocycle being optically substituted); X1 and X2 may be the same or different and are each an oxygen atom, a sulfur atom, or NR3; Y is CO, CS, CNR4, -CR5R6-, -CR5R6CR7R8-, or CR5R6CR7R8CR9R10-; one of R5 to R10 together with R3 may form an optionally substituted heterocycle; Z is a chalcogen atom or NR11; and the broken line represents a single bond or a double bond.
CN103536620A Azlocillin sodium composition powder for injection The invention provides an azlocillin sodium composition powder for injection, and belongs to the field of medicine and medicine preparation technology. The azlocillin sodium composition powder comprises following raw material ingredients, by weight, 7.26 to 9.17 parts of azlocillin sodium, 1.45 to 1.84 parts of chitosan nanoparticle, and 88.99 to 91.29 parts of injection water. Advantages of the azlocillin sodium composition powder are that: the size of the chitosan nanoparticle is ultra small, so that the chitosan nanoparticle is capable of passing through capillary vessels with a smallest diameter, rapid removing of the chitosan nanoparticle by macrophage is avoided, so that lasting time of the azlocillin sodium composition in blood is prolonged greatly; the azlocillin sodium composition is capable of improving antimicrobial activity of azlocillin sodium significantly, reducing dosage of azlocillin sodium in clinic, and reducing adverse reaction of azlocillin sodium; and the chitosan nanoparticle can be used as a freeze-dried skeleton agent of the freeze-dried powder injection instead of mannitol so as to avoid active effects of mannitol on human bodies.
CN102391164A Diaryl thioether compound, preparation method and application of thereof in tumor resistance The invention relates to the field of the development of new medicines, and relates to the field of the development of new medicines of anti-tumor medicines, in particular to a compound. A structure of the compound is shown as a general formula I, wherein A is selected from 4- nitro-substituted phenyl shown as a structural formula II, 4-alkoxy substituted phenyl shown as a structural formula III and a substituted heterocyclic ring shown as a structural formula IV or a structural formula V, and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are selected from hydrogen, halogen, hydroxyl, amido, substituted amio, cyan, alkyl, alkoxy, nitryl, acylamino, halogenated alkyl, acyl, formyl, carboxy, carbalkoxy or substituted alkyl having 1 to 3 carbon atoms independently, and R5, R6, R7 and R8 are not the hydrogen simultaneously; R9 is selected from alkyl having 1 to 3 carbon atoms or substituted alkyl having 1 to 3 carbon atoms; and X and Y are selected from nitrogen, oxygen or sulphur independently. The compound has the effects of resisting abnormal neovascularization and inhibiting the polymerization of microtubulin and has the advantages of high activity and low toxicity.
WO2008051282A3 Crystalline forms of 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno(2,3-d)pyrimidine The present invention is directed to novel crystalline forms of 4-(2-fIuorophenyl)-6-methyl-2-(piperazin-l-yl)thieno[2,3-d]pyτimidine salts, including 4-(2- fluorophenyl)-6-methyl-2-(piperazin- 1 -yl)thieno[2,3-d]pyrimidine hydrochloride crystalline forms. The present invention is also directed to compositions including such crystalline forms and methods for making and using such crystalline forms, e.g., in the treatment of gastrointestinal and/or genitourinary disorders.
US7465444 Methods of suppressing or treating an inflammatory bowel disease by administering an antibody or portion thereof that binds to AILIM Antibodies against AILIM (also called ICOS and 8F4) were found to significantly suppress the onset of inflammatory bowel diseases (especially Crohn's disease and colitis (ulcerative colitis and such)), and exhibit a significant therapeutic effect against inflammatory bowel diseases.
US20110136798 Crystalline Forms Of A Pyridine Derivative The invention relates to 4-methylbenzenesulfonate salt of the compound of formula (I) in a crystalline form or a solvate thereof, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.
US20100189779 In vivo device, system and usage thereof An in vivo device (1) for an at least temporary placement in a human or animal body (17), comprising an actuator (2) adapted to be actively triggered from the exterior in order to induce a local impact on the adjacent body area for in vivo treatment of a patient in need, and/or comprising a sensor adapted to be actively triggered from the exterior for sensing a pathological condition in the body (17). An in vivo system comprises at least two and/or a plurality of the in vivo devices (1), wherein the in vivo devices (1) are adapted to communicate with each other and/or with an external controller (24). The use of the in vivo device/s (1) for treating and/or diagnosing a pathological condition in a human or animal body (17) comprises: administering the device/s (1); monitoring the movement of the device/s (1) through the body (17); triggering the device/s (1) from the outside once the device/s (1) reach/es a defined position in the body (17).
US8436148 Antibodies against interleukin-18 binding protein, their preparation and use Interleukin-18 binding proteins which are capable of binding IL-18 and/or modulating and/or blocking IL-18 activity are provided. Methods for their isolation and recombinant production, DNAs encoding them, DNA vectors expressing them, vectors useful for their expression in humans and other mammals, antibodies against them are also provided.
WO2008065500A3 Heteroaryl amides as type i glycine transport inhibitors The present invention relates to a series of substituted heteroaryl amides of the Formula (I), wherein, R1-R12 groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, Including humans, wherein HET is a 5 or 6 membered membered heteroaryl ring optionally substituted by one or more substituents selected from R5; X1 Is C(=O) Or SO2;. X2 Is -(Czero-C1O alkyleneXO)y-(Czero-C10 alkytene)-, or -(C3C10 cycloalkyl)-(Czero-C10 alkylene)-(O)y-(Czero H10 alkylene)-; wherein y is O or 1; X3 Is -(Czero-C1O alkylene)-NR1R2; -(C3-C10 alkylene)-NR1R2; -(Czero-C10alkylene)-X4 or (C3-C10 cycloalkyl)-(Czero-C10 alkylene)-X4; wherein said cycloalkyl is optional substituted by one or more -OH; X4 is a nitrogen containing (5-15 membered) heterocydoalkyi or a nitrogen containing (5-15 membered) heteroaryl, each optionally substituted by one or more substituents selected from R5; with the proviso that the 4-15 membered heterocydoalkyi of X4 is not a 3-aza-bicyclo{3.1.0]hex-6-yl group; Ring A Is a -(C5-C15) aryt, -(5-15 membered) heteroaryl or (5-15 membered) heterocydoalkyi.
CN102399256A Glycyrrhetinic acid derivatives and preparation method, medicinal composition and application thereof to preparation of antitumor drug The invention provides glycyrrhetinic acid derivatives and medically acceptable salt thereof in a general formula (I) and a general formula (II). In the general formulas (I) and (II), R1 represents H, substituted or unsubstituted C1-C4 alkyl, C1-C4 alkenyl, alcyl alkyl, heterocycle alkyl, aryl, ceteroary, monosaccharide or polysaccharide, amino acid and polypeptide residue; R2 represents H, CH3, CH2CH3 or CH(CH3)2; R3 represents H, CH3CO, C2H5CO, C3H7CO, CF3CO and C6H5CO; and the salt comprises hydrochloride, hydrobromide, phosphate, lactate, tartrate, salicylate, sulfate, oxalate, acetate, succinate, maleate, malate, gluconate, toluenesulfonate, citrate, fumarate, formate and phenpropionate. The invention also provides a preparation method, a medicinal composition and application of the glycyrrhetinic acid derivatives. The glycyrrhetinic acid derivatives have a good anticancer effect.
CN102731458A Bi-isopentene coumarin, as well as preparation method and application thereof The invention discloses bi-isopentene coumarin, as well as a preparation method and application thereof. A new compound is separated from Micromelum falcatum, and is bi-isopentene coumarin shown in a formula (I). The LD50 (median lethal dose) value of the compound to artemia is 25.5mu g/mL, the anti-adhesion activity concentration IC50 (half maximal inhibitory concentration) of the compound to kentrogon is 6.77mu g/mL, and the half maximal inhibitory concentration IC50 of the compound to lung cancer cells HvEvc is 76.4mu g/mL. Therefore, the compound can be used for preparing an anti-artemia medicament, a fouling organism larva adhesion prevention medicament and an anti-tumor medicament or used as a leading compound, and has wide application prospect.
EP2576537A1 2 -amino- pyrimidine derivatives useful as inhibitors of jnk Compounds of formula I or pharmaceutically acceptable salts thereof, wherein R5 is a group of formula (a) or (b): and wherein m, n, p, q, X, Y, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity.
US7189739 Antiinflammatory agents; cardiovascular disorders; rheumatic disorders The invention is directed to compounds of the formula and the pharmaceutically acceptable salts thereof wherein Ar1 is indole, benzimidazole, or benzotriazole, optionally substituted with lower alkyl (1–4C), halo, or lower alkoxy (1–4C); X1 is CO or an isostere thereof; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl; n is 0 or 1; Z is CH or N; X2 is CH, CH2 or an isostere thereof; and Ar2 consists of one or two phenyl moieties directly coupled to X2 and optionally substituted by halo, nitro, alkyl (1–6C), CN or CF3, or by RCO, COOR, CONR2, NR2, OR or SR, wherein R is H or alkyl (1–6C) or by phenyl, itself optionally substituted by the foregoing substituents; with the proviso that if Z is N, X1 is CO, and Ar1 is indole, Ar1 must be coupled to X1 through the 2-, 5-, 6- or 7-position. These compounds are useful in the treatment of conditions associated with inflammation. In addition, the above compounds and other compounds described herein are useful in treating conditions associated with cardiac failure.
US7358261 Heteroaryl alkylamide derivatives useful as bradykinin receptor modulators This invention is directed towards novel alkylamide derivatives as bradykinin receptor antagonists useful for the treatment of bradykinin modulated disorders such as pain, inflammation, asthma and allergy. Furthermore, the present invention is directed to novel alkylamide derivatives as bradykinin receptor agonists useful for the treatment of bradykinin modulated disorders such as hypertension and the like.
CN103193772A Preparation method and application of substituted aryl propionic berberine ion-pair compound The invention relates to a preparation method and an application of a substituted aryl propionic berberine ion-pair compound. The substituted aryl propionic berberine ion-pair compound prepared by adopting the preparation method can be prepared into tablets, capsules, injections and gels and can be also prepared into suppositories applied to one part of the rectum and the vagina and lotions. The medicinal preparation prepared from the substituted aryl propionic berberine ion-pair compound has the effects of resisting bacteria, inflammation, cardiac failure and platelet aggregation, lowering blood pressure and treating hypertension, peptic ulcer and diabetes. The substituted aryl propionic berberine ion-pair compound has the pharmacological effect of the berberine hydrochloride and the pharmacological effect of the aryl propionic anti-inflammatory medicament.
US20050147665 Consisting of eicosapentaenoic acid or derivative, vitamin B 12, folic acid, at a maximum daily dose of 5 mg, and vitamin B6, at a maximum daily dose of 20 mg, and optionally at least one antioxidant; treatment of psychiatric disorders; schizophrenia, Alzheimer's disease, dementia, Parkinson's disease The combined application of at least one essential fatty acid of the n-6 or n-3 series, optionally together with further essential fatty acid(s) of the n-6 or n-3 series, together with one or more homocysteine lowering agent. The homocysteine lowering agent is selected from vitamin B12, folic acid, a compound related to folic acid with similar biological activity and vitamin B6.
CA2342830C 5-heterocyclyl pyrazolo[4,3-d]pyrimidin-7-ones for the treatment of male erectile dysfunction The invention is directed to novel substituted 5-heterocyclyl pyrazolopyrimidinones and derivatives thereof, their synthesis and their use in treating sexual dysfunction in mammals, especially male erectile dysfunction. Pharmaceutical compositions containing the compounds and methods of using them to treat sexual dysfunction are also described.
WO2005027951A1 Method for controlling angiogenesis in animals Disease conditions which are dependent upon or moderated by angiogenesis are controlled by the use of a therapeutic material which interacts with cell surface galectins. Particular therapeutic materials comprise a polymeric backbone having side chains terminating in a sugar dependent therefrom. Disclosed are specific therapeutic materials in which the polymeric backbone is based upon polygalacturonic acid, and the side chains terminate in arabinose or galactose.
US7101990 Bax-responsive genes for drug target identification in yeast and fungi The use of nucleic acids and polypeptides which are involved in a pathway eventually leading to programmed cell death of yeast or fungi for the preparation of a medicament for treating diseases associated with yeast or fungi or for the treatment of prolifeative disorders or for preventing apoptosis in certain diseases is disclosed. Methods are provided to identify compounds which selectively modulate the expression or functionality of said polypeptides in the same or a parallel pathway. Also provided are compounds as well as pharmaceutical compositions, medicaments and vaccines. New nucleic acid sequences, probes and primers derived thereof, expression vectors and host cells transformed with said vectors, polypeptides and antibodies raised against said polypeptides are also disclosed.
US7425623 Binding to surface of tumor cell; bacteriophage separation; in situ diagnosis A binding structure which binds in, and/or to the surface of, tumour cells; a target structure displayed and/or expressed in, or on the surface of, tumour cells; a binding structure that recognises and blocks said target structure; a substance that binds to or blocks the expression of said target structure; pharmaceutical compositions comprising said binding structure, target structures or substance as active principles; vaccine compositions comprising said target structures as active principles; a method for phage selection; and methods of in vitro and in vivo diagnosis and prognosis, and of treatment of human malignant diseases comprising the use of the above subject matters, are described.
CN101475556B 1',2',3',7'-tetrahydrotheaflavine, and preparation and use thereof The invention provides a novel compound, which is 1',2',3'7'- tetrahydro theaflavin and the chemical structural formula thereof is shown as (1). The compound of the invention can be obtained by hydrogenating and reducing theaflavin-TF1, has the functions of inhibiting the activity of reverse transcriptase and the activity of HIV gp41 forming a six-strand helical core structure, can prevent HIV virus from entering a host cell, and has stronger inhibiting functions on the activity of the reverse transcriptase and the activity of HIV gp41 forming the six-strand helical core structure than the theaflavin- TF1.
US20090099122 USE OF CpG OLIGODEOXYNUCLEOTIDES TO INDUCE EPITHELIAL CELL GROWTH This disclosure provides a method of inducing epithelial cell growth. The method includes administering an effective amount of a K-type CpG oligonucleotide, thereby inducing epithelial cell growth. The epithelial cell can be in vivo or in vitro. Methods are also provided for inducing wound healing in a subject. The methods include administering to the subject a therapeutically effective amount of at least on K-type CpG ODN.
US20080124411 nasal strip; and an orally administered composition comprising a tissue-firming agent, a tissue-soothing agent, a tissue lubricant, and an expectorant; for combating snoring An orally administered composition for relieving or eliminating snoring is described. The composition generally has four mechanisms of action for combating snoring. The composition includes a tissue-firming or astringent agent to firm up throat tissue. The composition also includes a soothing agent to soothe irritated or inflamed tissues. Also included in the composition is a lubricant to moisten dry or dehydrated tissues, and a mucous-thinning or expectorant agent to help remove any obstructive matter near the throat tissues.
CA2342804C Vending machine A vending machine (10) including a cabinet (12) having therein a storage compartment (21) and product extraction means (20) including a base (29) operatively connected to the cabinet for pivoting about vertical axis (27), first link means (25a) horizontally pivoted to the base, second link means (25b) horizontally pivoted to the other end of the first link, actuators for respectively pivoting the base, first link and second link, and coupling means operatively connected (through guide head (33)) to the other end of the second link means (25b) for coupling with a selected product in the storage compartment (21) for delivery to a product station, the extraction means (20) being controlled by control means (15) after product selection by a customer.
EP2776405A1 2-thiopyrimidinones Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
DE20320991U1 Use of palonosetron in the treatment and prevention of chemotherapy and radiotherapy-induced acute and delayed emesis Treatment of chemotherapy or radiotherapy-induced acute and delayed emesis involves administration of palonosetron (P1). - ACTIVITY : Antiemetic. The antiemetic efficacy of palonosetron (P1) against chemotherapy-induced emesis was evaluated in dogs treated with cisplatin (intravenous dosage of 3 mg/kg). The dogs were administered with (P1) (test) at intravenous dosage of 0.1 mg/kg or vehicle (control) 10 hours prior to administration of cisplatin. The emetic episodes were found to be 9.83+-4.79/19.33+-5.68 in test/control. The results also showed that (P1) protected even when administered 1 hour prior to administration of cisplatin and even at doses as low as 0.3 mg/kg. - MECHANISM OF ACTION : 5-Hydroxytryptamine receptor antagonist.
US20130045262 Sedative for external use, and sedative sheet, and textile, clothing, wall material, and hyperthermia equipment, brain vitalization sheet, brain vitalization small pillow Disclosed are a sedative for external use, and sedative sheet, and textile, clothing, wall material, and hyperthermia equipment, brain vitalization sheet, brain vitalization small pillow which are with high productivity, adaptive for various shape and various treatment style for patients with pain, and with high treatment effect, comparing with conventional sedative for external use. A sedative for external use 10 is provided which is a bag 2 containing desert rose powder 1 prepared by pulverizing desert rose.
EP1887003A1 3-[4-heterocyclyl -1,2,3-triazol-1-yl]-n-aryl-benzamides as inhibitors of the cytokines production for the treatment of chronic inflammatory diseases Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
CN1907294A Compound recipe copper sulfate cold cream The invention discloses a compound cupric sulfate cold cream to treat leukoderma in the medical technological domain, which is composed of cupric sulfate, glucocorticoids clobetasol propionate, transdermal accelerant and cold cream base. Because cupric sulfate and glucocorticoids clobetasol propionate are prepared into composite preparation, better treatment effect, quicker function and lower toxic action can be achieved when the local concentration is much lower than that of the single preparation of cupric sulfate and glucocorticoids clobetasol propionate.
CN103405473A Mixed carbohydrate-electrolyte injection and preparation method thereof The invention belongs to the field of a pharmaceutical preparation, and particularly relates to a mixed carbohydrate-electrolyte injection and a preparation method thereof. A pH modifier of the injection is citric acid, and pH is 4.0-4.4. By controlling the dosage range of the pH modifier, the pH range of the finished product can meet the specification only by regulating the pH value for one time in the preparation process. In addition, according to the method, activated carbon is added only in the step, and the activated carbon is not added in the preparation process, so that the risk of introducing metal ions and other impurities through the activated carbon can be effectively avoided, and toxins in bacteria of the finished product are qualified. According to the method, the technology is further simplified, the production time and cost can be shortened and lowered, and the sterilized product has no crystallization or precipitation phenomenon. After being stored for 24 months, the 5-hydroxymethyl-furfural range of the injection is within 0.03-0.05, and the impurities are controlled at the extremely low level; after being stored for 24 months, the injection almost has no character change and is still colorless clear liquid compared with the injection which is stored for zero day.
WO2012107455A1 Galactofructose for the regulatory effect thereof on intestinal transit Galactofructose for the regulatory effect thereof on the intestinal transit time of mammals, when it is incorporated into a food composition and when the latter is absorbed by the mammal in an amount corresponding to daily doses of galactofructose, averaged over 30 days, of between 0.1 and 2 g.
US20100298421 Derivatives of taxol and closely related compounds A cytotoxic composition in which two moieties are conjugated covalently. A first moiety is a tax moiety, selected from the group consisting of taxanes, taxane derivatives, and or other closely relative compounds. A second moiety is an acid moiety selected from the group consisting of lipoic acid, acetylcysteine, compounds having an acidic group.
WO2006034085A1 Crystalline form of atrasentan hydrochloride Substantially amorphous atrasentan hydrochloride, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
WO2012150340A1 Compounds for use in the treatment of filariasis The present invention relates to compounds according to the general formula (1) for use in the therapeutic or prophylactic treatment of filariasis, a nematicidal composition comprising as an active ingredient a compound according to the general formula (1), and a method for treating filariasis.
CN102205021A Collateral-moistering bone-penetrating oil A collateral-moistering bone-penetrating oil mainly has the following efficacy of: dispelling wind and activating blood, reducing swelling and relieving pain, relieving arthralgia and dredging collaterals, clearing heat and removing toxicity, and arresting convulsion. The collateral-moistering bone-penetrating oil is used to treat rheumatalgia, muscle and bone pain, arthralgia, quadriplegia, hemiplegia, soreness and pain in loins and legs, sciatica, periarthritis pain, toothache, stomachache, cold, various swelling and pain by traumatic injury, scabies, leprosy, and infantile convulsion. The invention is mainly based on the following preparation method which comprises: according to a formula dosage, pulverizing 100-150 g of each of hedyotis diffusa, scorpion, centipede, and leeches, 50 g of bamboo bees, 15-20 g of each of panax notoginseng, myrrh, frankincense, angelica, and banksia rose, 200-350 g of each of patchouli, licorice, star anise, cinnamon, tangerine peel, cape jasmine, mint, ligusticum wallichii, safflower, moghania philippinensis, and dragons blood into powder, adding a proper amount of mint oil and clove oil, stirring uniformly, soaking at a room temperature of 18-25 DEG C for 30 days; filtering the mixed solution, keeping the filtrate in reserve; adding 60-80 g of menthol, 30-40 g of camphor, 15-20 g of borneol, 30-40 g of each of cassia oil, eucalyptus oil, sweet basil oil, litsea cubeba oil, wintergreen oil, clove oil, and cassia leaf oil into the obtained filtrate, stirring uniformly, adding 50 g of clove oil and 1000 g of mint oil, mixing well, sealing and storing the mixture in a dark and cool place for 49 days to obtain a finished product. The using method is: externally applying the oil to an affected part till heat is generated.
CN103169684A Ilaprazole enteric orally disintegrating tablet and preparation method thereof The invention relates to an ilaprazole enteric orally disintegrating tablet and a preparation method thereof. The ilaprazole enteric orally disintegrating tablet comprises the components in percentage by weight as follows: 1-5% of ilaprazole, 8-10% of hollow pill core, 2-5% of stabilizer, 10-15% of isolating layer, 15-20% of enteric coating, 35-70% of filler and 10-20% of disintegrating agent. The invention provides the ilaprazole enteric orally disintegrating tablet which is small in grain size, quick to absorb, high in bioavailability, good in taste, easy to swallow, good in disintegrating effect, strong in compressibility and convenient for patients to take, and the preparation method thereof.
CN103058935A Pyrimidine compound as well as preparation method and use for same The invention provides a pyrimidine compound or the pharmaceutically acceptable salts thereof. The invention further provides a preparation method and use for the same. The pyrimidine compound provided by the invention has an inhibition effect on both tumour cells and viruses, and is especially good in the effects of resisting colon cancer, flu and herpes viruses, thus providing a new choice for clinical medication.
US20080009495 Compound Containing Basic Group and Use Thereof The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
US20050221303 Sequences involved in phenomena of tumour suppression, tumour reversion, apoptosis and/or virus resistance and their use as medicines This invention is directed to sequences that are involved in the molecular pathways of tumor suppression, tumor revision, apoptosis and/or virus resistance. The use of the compounds having these sequences, or encoded by them, in treating cancer, neurodegenerative diseases or viral diseases, and screening methods for compounds having such therapeutic properties are also encompassed.
US20050065139 Antidiabetic agents; controlling carbohydrate metabolism A method for synthesizing Salacinol, its stereoisomers, and analogues, homologues and other derivatives thereof potentially useful as glycolsidase inhibitors. The compounds of the invention may have the general formula (I) or (II): The synthetic schemes comprise reacting a cyclic sulfate with a 5-membered ring sugar containing a heteroatom (X). The heteroatom preferably comprises sulfur, selenium, or nitrogen. The cyclic sulfate and ring sugar reagents may be readily prepared from carbohydrate precursors, such as D-glucose, L-glucose, D-xylose and L-xylose. The target compounds are prepared by opening of the cyclic sulfates by nucleophilic attack of the heteroatoms on the 5-membered ring sugars. The resulting heterocyclic compounds have a stable, inner salt structure comprising a heteroatom cation and a sulfate anion. The synthetic schemes yield various stereoisomers of the target compounds in moderate to good yields with limited side-reactions.
US20100113610 Methods for controlling inflammatory and immunological diseases The present invention provides methods for generating mucosal tissue homing immunosuppressive T-cells comprising treating naïve T-cells with retinoids and/or retinoid agonists. Methods are also provided for treating a mammal having an inflammatory or immunological disease by administering a therapeutically effective dose of retinoids and/or retinoid agonists. Additional methods are also provided for boosting the immune system of a mammal by inhibiting the generation of immunosuppressive T-cells by administering a therapeutically effective dose of a retinoid receptor antagonist to the mammal.
US20120129794 Apparati, methods, and compositions for universal microbial diagnosis, detection, quantification, and specimen-targeted therapy Microbial ecology of a specimen is evaluated using an approach (Level I) that utilizes nucleic acid amplification with specific gene primers that will identify panels of microorganisms and antibiotic-resistance factors generating a diagnostic report (optionally with quantification of each microorganism or antibiotic-resistance factor) and an approach (Level II) that utilizes universal or semi-universal primers to amplify conserved genes at a general or specific taxonomic level that are tagged specimen specifically using a genetic or chemical marker that is specific to the specimen from which it was derived, then sequencing the amplified products with highly-parallel, high-throughput technology to provide comprehensive sequences of the microbial population in the specimen followed by analysis of this sequence information and specific targeted information from Level I and/or Level II to generate a comprehensive analysis, interpretation, and/or diagnostic report.
US7335376 Method for photodynamic therapy and applicator for carrying out said therapy The present invention relates to medicine, more concretely to photodynamic therapy, and may be used in oncology and dermatology. A method is proposed for photodynamic therapy of pathological surface formations, which comprises sensitizing a surface of the pathological area by superposing an applicator containing 5-aminolevulinic acid, and irradiating the sensitized area with therapeutic optical radiation in the spectral range of 625-700 nm, wherewith an applicator is used which is transparent in the spectral range of at least 625-700 nm, and irradiation is carried out through the applicator. Wherewith therapeutic irradiation is carried out under control of the intensity of fluorescence of the tissues of the pathological area by irradiation of the tissues in the spectral range of 625-635 nm and measurement of the intensity of fluorescence in the range of 635-700 nm through the applicator. In the method an applicator may be used which is also transparent in at least one of the spectral ranges 390-460 nm, 510-540 nm or 570-590 nm. The applicator used in the proposed method consists of a base of a bioinertial material and a sensitizing layer including a carrier and 5-aminolevulinic acid dissolved or dispersed in the carrier. The base is made in the form of a film of a bioinertial polymer, transparent in the spectral range of at least 625-700 nm, and the carrier is made in the form of a film layer of biocompatible hydrophilic terpolymers of N-vinylpyrrolidone, amide of acrylic acid and of ethyl ether of acrylic acid with a ratio of the monomeric links respectively (20-35):(35-60):(20-30) wt. % and a molecular weight of from 20 000 to 1 000 000 Daltons. The bioinertial polymer may also be transparent in at least one of the spectral ranges of 390-460 nm, 510-540 nm or 570-590 nm. This polymer is regenerated cellulose, polyethylene terephthalate or a polyamide. The proposed method for photodynamic therapy and the applicator for implementation of the method make it possible to enhance the efficacy of photodynamic therapy and reduce the expenditure of 5-aminolevulinic acid.
CN101186598A 1-oxy-acetyl inula Britannica lactone derivative, preparation method thereof and application of the same in preparing cancer-curing medicine The invention discloses a 1-oxygen-acetyl-hana-flowered-lactone derivative, relative preparation method and relative application in the drug preparation for treating cancer. The inventive preparation method comprises that 1-oxygen-acetyl-hana-flowered-lactone is directly condensed with relative acyl chloride to obtain product, or in the presence of catalytic condenser, 1-oxygen-acetyl-hana-flowered-lactone and relative acid are directly dewatered and acylated to obtain product. The inventive 1-oxygen-acetyl-hana-flowered-lactone derivative has significant cancer resistant activity, while the drug agent which active component is the inventive compound can be used for cancer treatment or cancer adjuvant treatment, in particular for leukemia, liver cancer and lung cancer.
US20070248672 Indole and Azaindole Derivatives with Antitumor Action Indole and azaindole compounds useful for the treatment of solid tumours and tumours of the blood are described, they being particularly effective in the treatment of drug resistant tumours; these compounds are also able to synergistically enhance the activity of known antitumour drugs. They can hence be used either alone as antitumour agents or in association with known antitumour drugs. Processes for preparing the aforesaid compounds, which are partly new, and pharmaceutical compositions useful for the aforesaid treatments are also described.
WO2006021656A2 Aminopiperidine derivatives, preparation thereof and use thereof as melanocortin receptor agonists The invention concerns aminopiperidine derivatives of general formula (I) wherein: Ra, Ra' and R5 represent hydrogen atoms or alkyl groups; R1 represent a hydrogen atom and an alkyl, cycloalkyl, heterocycloalkyl or aryl group; R2 represents a group of formula -(CH2)x-(CO)y-Y or -(CO)y-(CH2)x-Y, wherein Y represents a hydrogen atom or a hydroxy, alkyl, cycloalkyl, alkoxy, aryl, heteroaryl or NR 11R12 group, Y being other than a hydrogen atom when x = y = 0; R3 represents 1 to 3 groups selected among halogen atoms and alkyl, cycloalkyl, -OR, -NRR', -CO-NRR', -NR-CO-R', -NR-CO-NRR', -NR-COOR', -NO2, -CN and COOR groups; R4 is selected among groups of formula (a), (b) and (c), wherein p = 0, 1, 2 or 3, m = 0, 1 or 2; X represents an oxygen or sulphur atom or a -C(R 6)(R7)- or -N(R10)- member. The invention also concerns a method for preparing said derivatives and their therapeutic use as melanocortin receptor agonists for treating obesity, diabetes, sexual dysfunction.
CA2338252C Composition for enhancing lipid production, barrier function, hydrogen peroxide neutralization, and moisturization of the skin Increased production of skin lipids, increased barrier function, hydrogen peroxide neutralization, prevention of loss of the natural moisturizing factor from the stratum corneum and moisturization of the skin is provided by a topically applicable composition which includes one or more components selected from the group consisting of branched chain amino acids, derivatives of branched chain amino acids and mixtures thereof, which one or more components are capable of being catabolized in epidermal cells to form lipid precursors for epidermal lipid synthesis. The composition can also include one or more enzyme activators which increase the rate of catabolism of the one or more components.
CN101108164A Bcg polyoses nucleic acid intralipid and its cryochem formulated product and use thereof A bcg polyoses nucleic acid intralipid and its freeze dehydration agent and purpose are provided. The proportion for the weight shares of intralipid is: bcg polyoses nucleic acid of 0.05 to 0.5 per cent, oily component of 4 to 8 per cent, emulsifier of 3 to 8 per cent and water of 84 to 92 per cent. The oily component refers to one or more than one from plant oil, animal oil, neutral lipids, synthetic grease, sterol derivative; the emulsifier refers to the normative emulsifier in making medical preparation with the pH value of preparation liquid of 6.5 to 7.5; freeze and dry the intralipid under normal condition to make freeze dehydration agent. The invention can be applied as therapeutic agent for resisting cancer, intra-cellular infection, hypersusceptibility, cold and asthma. In the invention, the biologic reaction regulator of bcg polyoses nucleic acid is prepared as a lymph targeting preparation that can effectively regulate immunity, resisting cancer, intra-cellular infection, hypersusceptibility, cold and asthma with high efficiency and without toxic content.
US20050124646 Tricyclo compounds, a process for their production and a pharmaceutical composition containing the same This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases, infectious diseases, and the like, which can be represented by the following formula: to a process for their production, to a pharmaceutical composition containing the same and to a use thereof.
US20110237537 Methods for assessment and treatment of mood disorders via single nucleotide polymorphisms analysis Described herein are assays, kits and methods for treating mood disorders by testing for one or more polymorphisms in a specific group of genes and for analyzing the results of polymorphism testing; the genes included may converge in one or more signaling pathways, and may be epigenetic. The genes are included based on the relationships of the proteins encoded by the genes in the context of particular signaling pathways and provide a diagnostically relevant nexus. Also described herein are methods of presenting the data collected by the screen, including methods of delivering interpretive comments and/or treatment guidance based on the results of the genetic screening either individually or based on the genetic composition of particular clusters of genes which may be related to each other. Importantly, drugs which modulate these genetic disturbances are described for targeted therapeutic use based upon companion diagnostic method.
WO2011162480A9 Composition for treating prion diseases comprising hif-1α agonist The present invention relates to a pharmaceutical composition and a veterinary composition for preventing and treating prion diseases which comprises an HIF-1α agonist as an active ingredient. More specifically, HIF-1α, whose expression is increased in a low oxygen state, alleviates the cytotoxicity which modified prion protein peptides have against nerve cells and so effectively suppresses cell death and increases the expression of normal prion proteins, such that it can be used as an agent for treating prion diseases or as a feed additive for relieving prion diseases.
WO2005082349A1 Composition for the treatment of obesity comprising fumagillol derivative Disclosed herein is a composition for the treatment of obesity which comprises a compound selected from the group consisting of O-(4-methoxycinnamoyl)fumagillol, O-(3,4,5-trimethoxycinnamoyl)fumagillol, O-(4-dimethylaminoethoxycinnamoyl)fumagillol, and salts thereof; and a pharmaceutically acceptable carrier. Since the composition potently inhibits the proliferation and increases the apoptosis of vein endothelial cells in adipose tissues to reduce the adipose tissues, and decreases food intake to cause weight loss, it shows superior therapeutic effects on obesity with few or no side effects.
DE102006053690A1 New anionic cyclopentadienyl-carbohydrate compounds useful in the preparation of metallocene-carbohydrate compound, which is useful to treat cancer Anionic cyclopentadienyl-carbohydrate compounds (I), are new. Anionic cyclopentadienyl-carbohydrate compounds of formula (I), are new. m : 0-10 (preferably 1); ER1 : OH, alkoxy, nucleo-base or N-alkylated nucleo-base, preferably methoxy or N-methyl-uracil; either R4a-R4d : H (preferred) or alkyl; or R4a+R4b+R4c+R4d : aromatic, olefinic and/or aliphatic carbo- or heterocyclic form; and R2, R3 : H or alkyl (preferably -CH 2- or -C(CH 3) 2-), where R2 and R3 are optionally alkylene. Where OR2 and OR3 are cis to each other. Independent claims are included for: (1) a metallocene-carbohydrate compound of formula ((I) n-MXY1-(II) 2 - n) (A); and (2) the preparation of metallocene-carbohydrate compound comprising reacting a carbohydrate in the furanose form with (I), where the carbohydrate shows the following features: the glycosidic OH-group is protected or is bonded in place of nucleobase or N-alkylated nucleobase to form a furanose ring, the further both OH groups bound directly at the furanose ring are protected and the exocyclic, was transported over a methyl group with the furanose ring connected OH-group in a leaving group accessible for nucleophilic substitution, deprotonating the obtained carbohydrate-cyclopentadiene-compound, and transmetallizing the obtained carbohydrate cyclopentadienyl salt with a mediator compound of scandium, yttrium, lanthanum, titanium, zirconium, hafnium, vanadium, niobium, tantalum, chromium, molybdenum, tungsten, manganese, technetium, rhenium, iron, ruthenium, osmium, cobalt, rhodium, iridium, nickel, palladium, platinum, copper, silver, gold, zinc, cadmium or mercury. M : Sc, Y, La, Ti (preferred), Zr, Hf, V, Nb, Ta, Cr, Mo, W, Mn, Tc, Re, Fe, Ru, Os, Co, Rh, Ir, Ni, Pd, Pt, Cu, Ag, Au, Zn, Cd and/or Hg; X, Y1 : halo (preferably chlorine), alkoxy, alkyl, aryl, aryloxy, benzyl or benzoate; either R5a-R5e : H (preferred) or alkyl; or R5a+R5b+R5c+R5d+R5e : aromatic, olefinic and/or aliphatic carbo- or heterocyclic; and n : 1 or 2. [Image] [Image] - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : None given.
WO2014012859A1 Fumaric acid salt of 9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy- chinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one, its use as medicament and the preparation thereof The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.
WO2008020180A2 Methods of increasing the sensitivity of cancer cells to dna damage The present invention relates to the finding that cells which have a kinase-deficient phenotype have increased sensitivity to DNA damage promoting agents, in particular PARP inhibitors. Methods of treating cancers with a kinase-deficient phenotype using DNA damage promoting agents and methods of treating cancers with a combination of DNA damage promoting agents and kinase inhibitors are provided, along with screening methods for identifying new therapeutics for use in combination with DNA damage promoting agents.
WO2009068320A1 Aryl and heteroaryl fused imidazo (1,5-a) pyrazines as inhibitors of phosphodiesterase 10 The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.
EP2125773B1 Thiophene derivatives useful as medicaments for treating ocular hypertension Disclosed herein is a compound according to one of the formulas or a pharmaceutically acceptable salt thereof, medicaments for the treatment of glaucoma or ocular hypertension and compositions related thereto, as further elaborated herein.
WO2014070979A1 Inhibitors of cytomegalovirus Compounds of Formula (I) wherein n, R1, R1A, R2, R4 and Z are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
US20100291028 Use of il-18 inhibitors for treatment and/or prevention of peripheral vascular diseases The invention relates to the use of an inhibitor of IL-18 in the preparation of a medicament for treatment and/or prevention of peripheral vascular diseases. The invention further relates to the use of an IL-18 inhibitor for prevention of limb amputation.
US7211601 Prevention labor contraction; urogenital disorders The present invention is related to pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO22-, —SO2NH—, —CH2-, B is either a group —(C═O)—NR8R9 or represents a heterocyclic residue having the formula (a) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5–6 membered aryl or heteroaryl ring.
CN1736478A Composition for lowering blood fat The invention provides a composition for regulating blood fat, which comprises lactoferrin and tervalence chromic compound, the tervalence chromic compound is selected from at least one of 6H2O chromium trichloride, chromium trichloride, chromic acetate, chromic sulfate, arsenic chromic formate, niacin chromium or other inorganic trivalent chromium or organic trivalent chromium group. The invention also relates to a method for regulating receptor blood fat.
CN102085216A High-density calcium carbonate tablet and preparation method thereof The invention discloses a high-density calcium carbonate tablet and a preparation method thereof. The high-density calcium carbonate tablet contains high-compressibility and high-purity medicinal calcium carbonate particles and vitamins D3. The density of the calcium carbonate tablet is 1.85-2.1g/m<3>. The invention also discloses a preparation method of the high-density calcium carbonate tablet.
US20110118227 Methods for the Treatment of Fibromyalgia and Chronic Fatigue Syndrome The invention relates to methods for the treatment of fibromyalgia and chronic fatigue syndrome by administration of a transdermally applied androgen composition. The treatment is both safe and effective for treating fibromyalgia-related pain and fatigue, as well as chronic fatigue syndrome.
US7638546 Imidazolyl derivatives The present invention is directed to imidazolyl derivatives of formula (I) where the substituents are defined in the specification, which are useful as agonist or antagonists of somatostatin receptors.
WO2013007763A1 MODULATORS OF THE NLRP3 INFLAMMASOME IL-1ß PATHWAY FOR THE PREVENTION AND TREATMENT OF ACNE The invention provides inhibitors capable of binding to a member of the inflammasome group comprised of IL-1 β, IL-1 receptor type 1, NLRP3, ASC, Caspase-1 and cathepsin B with a dissociation constant of 10-8 mol/l or smaller for the prevention and treatment of acne, specifically an antibody, an antibody fragment, an antibody-like molecule, an oligopeptide of 6 to 30 amino acid residues, a nucleic acid aptamer molecule of 10 to 75 nucleotides in length or a soluble polypeptide comprising a contiguous amino acid sequence of at least 30 amino acids comprised within the protein sequence of a member of the group comprised of IL-1 β, IL-1 receptor type 1, IL-1 receptor type 2, NLRP3, ASC and Caspase-1. Similarly, an interfering RNA or an antisense modulator of gene expression of IL-1 β, I L-1 β receptor type 1, NLRP3, ASC, Caspase-1 and cathepsin B are provided for the prevention or treatment of acne.
US7323471 Administering azathioprine, 6-mercaptopurine, or 6-thioguanine nucleotide, or their salts for treating graft-versus-host disease of the mouth; oral rinse A method for treating or preventing symptoms associated with oral autoimmune diseases comprises treating a patient with an oral topical formulation of azathioprine or a pharmaceutically acceptable salt thereof. The azathioprine formulation may be used in the form of an oral rinse to topically treat areas of oral tissue inflammation and ulceration caused by the onset of oral autoimmune diseases, such as GVHD. The oral topical formulation of azathioprine may also be used in combination with other topical or systemic immunosuppressants or anti-inflammatory drugs.
CN101837084A Externally-used medicinal composite preparation for treating alopecia and manufacturing method thereof The invention discloses an externally-used medicinal composite preparation for treating alopecia and a manufacturing method thereof, which is an externally-used preparation prepared by mixing raw frankincense, raw myrrh, dragon's blood, cutch, agkistrodon halys, elephant hide (such as peccary skin), autumn tree branch, locust tree branch, willow branch, mulberry branch, gingko tree branch (or leaves), sesame oil and lead powder in a mass ratio. The preparation is made into plaster and spread on parts wherein hairs shed, and has the effects of activating blood, relieving pains, expelling wind, removing dampness, closing sores, engendering flesh, generating skin and growing hairs. The preparation is mainly used for treating alopecia areata, alopecia premature, beard and eyebrow loss and seborrheic alopecia. And the preparation has the characteristics of short treatment period, quick response and safe and convenient use.
US20130035322 Gold complexes Gold (I) hydroxide complexes of the form Z-Au-OH and digold complexes of the form Z—Au-(μOH)—Au—Z where groups Z are two electron donors are provided. The groups Z may be carbenes, for example nitrogen containing heterocyclic carbenes (NHCs), phosphines or phosphites. The complexes can be used as catalysts, for example in reactions such as hydration of nitriles, skeletal arrangement of enynes, alkoxycyclisation of enynes, alkyne hydration, the Meyer-Shuster reaction, 3,3′ rearrangement of allylic acetates, cyclisation of propargylic acetates, Beckman rearrangements and hydroamination. The complexes can be used in medicine, for example in the treatment of cancer.
WO2014131315A1 Bridged ring compounds as hepatitis c virus inhibitors, pharmaceutical compositions and uses thereof Provided herein is a compound of formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are a pharmaceutical composition comprising the compound and the use of the compound and the pharmaceutical composition thereof, which can also be used for treating HCV infection or a HCV disorder.
US8168647 Vinblastine derivatives, their preparation, use and pharmaceutical compositions comprising the said derivatives The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.
US20080027053 Antimicrobial oxazolidinone prodrugs This invention includes oxazolidinone prodrug compounds of Formula (I) and Formula (II) as defined herein. The prodrugs are convertible by natural biological processes into an active ingredient possessed of antimicrobial properties useful in treating bacterial infections in mammals.
EP1379508B9 N-(aryl)-2-arylethenesulfonamides and therapeutic uses thereof N-(Aryl)-2-arylethenesulfonamides and pharmaceutically acceptable salts and compositions thereof are useful as antiproliferative agents, including, for example, anticancer agents. They are also useful as radioprotective agents.
CN101189221B Ampa receptor potentiators The present invention relates to AMPA receptor potentiators of Formula (I), formulations comprising them, methods for their use, and intermediates useful for their preparation.
CN101518574A Anti-human papilloma virus (anti-HPV) external effervescent tablet and preparation method and application thereof The invention relates to an anti-human papilloma virus (anti-HPV) external effervescent tablet and a preparation method and application thereof. The anti-HPV external effervescent tablet comprises the following ingredients by the weight parts: 100 to 300 parts of anti-HPV medicinal powder, 150 to 300 parts of effervescing agent, 80 to 180 parts of diluting agent, 30 to 60 parts of disintegrant, 5 to 20 parts of lubricant and 70 to 90 parts of adhesive. The prepared anti-HPV external effervescent tablet has the advantages of favorable stability, convenient use, rapid disintegration, portability, and the like, has favorable treatment and prevention effects on genital benign or malignant diseases caused by affected HPV, can be used for preventing focal parts from recurring after a vulva, vagina or cervical carcinoma operation, has good water solubility, large foam number, uniform dispersedness and rapid curative effect, is suitable for washout or inunction according to a concentration standard and has the prevention effect on the early HPV infection of male and female genital tracts.
WO2008086483A2 Modulation of neurogenesis with use of modafinil The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasin neurogenesis. The disclosure includes compositions and methods based on use of modafinil, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.
WO2008010335A1 Plant extract having arthritis-preventive effect Disclosed is: an extract from a plant belonging to the family Compositae, preferably a plant Tanacetum parthenium, which contains a sesquiterpenelactone; or a beverage/food, quasi drug or pharmaceutical composition for prevention or treatment of a joint disease or a disease for which the inhibition of NFκB is effective, which comprises parthenolide. Also disclosed is a method for prevention or treatment of a joint disease or a disease for which the inhibition of NFκB is effective, which comprises feeding or administering an extract from a plant belonging to the family Compositae, preferably a plant Tanacetum parthenium, which contains a sesquiterpenelactone to a subject, or feeding or administering parthenolide to a subject.
EP1699468B1 Pharmaceutical composition comprising a zinc-hyaluronate complex for the treatment of multiple sclerosis The invention relates to pharmaceutical compositions for the treatment of multiple sclerosis which comprises a zinc-hyaluronan complex, preferably a zinc-hyaluronan complex with a molecular weight of 800-1200 kDa, as active ingredient and a pharmaceutically acceptable carrier and/or additive. The process for the preparation of said pharmaceutical compositions as well as the therapeutic use thereof for the treatment of multiple sclerosis are also within the scope of the invention.
EP1646380A2 Indolocarbazole anticancer agents and methods of using same The present invention relates to anti-tumor compounds, compositions and methods. In particular, the invention relates to indolocarbazole analogues of general Formulas (I) and (II) that inhibit topoisomerase I activity.
US20100056547 OPHTHALMIC COMPOSITIONS COMPRISING dDC A composition comprising dDC and a polymer, wherein the composition is an aqueous liquid with a viscosity which increases upon contact with a surface of an eye is disclosed herein. An aqueous composition comprising a therapeutically effective concentration of dDC, wherein the concentration of dDC is less than 1% is also disclosed. An eye drop comprising a therapeutically effective amount of dDC, wherein the amount of dDC is less than 300 μg is also disclosed. A method comprising administering an effective amount of dDC topically to an eye of a person suffering from viral conjunctivitis a viral infection, wherein less than 300 μL of dDC is administered to said eye is also disclosed. A kit comprising a composition and a dispenser, wherein said dispenser dispenses a drop comprising a therapeutically effective amount of dDC, wherein the amount of dDC is less than 300 μg is also disclosed.
US7166455 A genetic engineered nuclear acids, culturing Bacteroides fragilis, encoding immunomodulator, treating inflammatory bowel disease The present invention is directed to methods for producing and selecting novel mutant strains of B. fragilis that constitutively express a particular capsular polysaccharide or only selected capsular polysaccharides; compositions directed to the novel mutant strains of B. fragilis that constitutively express a particular capsular polysaccharide or only selected capsular polysaccharides; improved methods for purification of individual capsular polysaccharides; and compositions directed to novel res02 and inv19 genes and their gene products. Significantly, the present invention provides methods and compositions for overexpressing and purifying immunomodulatory capsular polysaccharide A (PSA) in high yield.
US7138521 Crystalline of N-[4-[2-(2-Amino-4,7-dihydro-4oxo-3H-pyrrolo[2,3-D]pyrimidin-5-YL)ethyl]benzoyl]-L-glutamic acid and process therefor The invention relates to the field of pharmaceutical and organic chemistry and provides an improved process for preparing the novel heptahydrate crystalline salt of multitargeted antifolate N-[4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid.
EP2376484A1 Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases.
WO2007124544A1 Integrase inhibitors - 1 The present invention describes a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Compounds of formula (I) are also provided.
WO2010078319A1 Lipoic acid containing compositions for use in the treatment and prevention of ki dney- related disorders in companion animals The invention encompasses compositions and their use for treating or preventing a kidney-related disorder in companion animals, wherein the compositions and uses include feeding the companion animal a composition including lipoic acid or a salt thereof.
WO2010081817A1 Method for treating colorectal cancer The present invention relates to a method of treating patients suffering from colorectal cancer characterized by coadministration of BIBF 1120 and BIBW 2992, wherein in said method BIBF 1120 is administered according to a continuous daily regimen and BIBW 2992 is administered according to a weekly alternating on-off regimen, pharmaceutical compositions and kits suitable for this method as well as their preparation.
WO2008051594A2 Anti-resorptive and bone building dietary supplements and methods of use Disclosed herein are dietary supplement compositions and methods for increasing or stimulating bone growth, decreasing or preventing bone resorption, increasing bone strength, improving bone structure, and improving bone architecture comprising a first composition comprising a combination of at least two of: quercetin, Rehmannia sp., Rehmannia sp. root, Siberian ginseng, Sophora japonica, licorice, and ipriflavone, wherein the combination of the first composition increases bone morphogenic protein-2 gene, promoter or protein expression; and a second composition comprising an extract of pomegranate in combination with at least one of Siberian ginseng, Ginkgo biloba, green tea, Sophora japonica, Rehmannia sp., grape seed, Dong Quai, and ipriflavone, wherein the combination of the second composition inhibits the expression of RANK-L.
US7153879 E.g., 7,11-Di(hydroxy)-8,8,10,12,16-pentamethyl-3-(1-methyl-2-(methylthiazol-4-yl)ethenyl)-4-aza-17-oxabicyclo(14.1.0)heptadecane-5,9-dione, preferably Form A; anticarcinogenic, -proliferative, -diabetic, -inflammatory agents; viricides; autoimmune diseases; psoriasis; agents; cardiovascular disorders There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.
US20120177719 Medical device intended to come into contact with a patient's tissue and related manufacturing method A device including a body (12) including fibers without oxidized cellulose. The body (12) also includes fibers containing oxidized cellulose.
EP2734535A2 2',3'-DIDEOXY-2'-alpha-FLUORO-2'-beta-C-METHYLNUCLEOSIDES AND PRODRUGS THEREOF The present invention provides 2',3'-dideoxy-2'-fluoro-α-2'-C- methylnucleosides, their prodrugs, and therapeutic use thereof as anti-HCV agents. The present invention also provides processes and intermediates for the preparation of the nucleosides disclosed herein.
EP1694673B1 Thiazole derivates The present invention relates to compounds of formula (I)wherein R1, R2, R3 and R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, for use as therapeutically active substances. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB 1 receptors.
CN101031558A HIV inhibiting 5-heterocyclyl pyrimidines HIV replication inhibitors of formula (I), 1=a2-a3=a4- is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; -b1=b2-b3=b4- is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; -S(=O)PR6; C(=NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; -CH=N-NH-C(O)-R16; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C 2-6 alkynyl; -C(=N-O-R8)-C1-4alkyl; R7 or -X3-R7; X1 is -NR1-, -O-, -C(=O)-, -CH2-, -CHOH-, -S-, -S(=O)P- R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; -CH=N-NH-C(O)-R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; -C(=N-O-R8)-C1-4alkyl; R7; -X3-R7 ; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy.
US7439244 e.g. 8-(4-(4-Fluorobenzyl)-piperazin-1-yl)-3-phenylsulfonylquinoline; serotonin receptor modulator; antidepressant, anxiolytic agent, cognition activator; schizophrenia, obesity, Alzheimer's disease Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other disorders.
US20100291221 Method of administering dose-sparing amounts of formoterol fumarate-budesonide combination particles by inhalation Disclosed are methods, and related compositions, that include administering a dose-sparing amount of a formulation that includes inhalation particles to a subject by inhalation; wherein the inhalation particles comprise formoterol fumarate and budesonide, the formoterol fumarate and budesonide being in a distributed encapsulated morphology with respect to one another within said inhalation particles and the formoterol fumarate being in a predetermined mass ratio with regard to the budesonide within said inhalation particles.
US20100022649 Pharmaceutical Composition and Procedure to Treat and Prevent Prostatic Hyperplasia and Prostatitis From the Royal Palm (Roystonea regia) Fruits A method for treating and/or preventing BPH prostatitis, alopecia and hirsutism including administering a medication of the pharmaceutical composition obtained from the green or mature fruits of Roystonea regia including a mixture of primary fatty acids with 8 to 28 carbon atoms, the fatty acid selected from the group consisting of caprilic acid (C8:0), capric acid (C10:0), lauric acid (C12:0), miristic acid (C14:0), palmitic acid (C16:0), palmitoleic acid (C16:1), stearic acid (C18:0), oleic acid (C18:1), linoleic acid, and linolenic acid and a mixture of esters of the fatty acids, and free fatty acids are enriched from ester hydrolysis.
CN103553919A Terpenoid and preparation method and application thereof The invention provides a terpenoid shown by the formula I or pharmaceutically acceptable salt, ester or hydrate thereof. The invention also provides a preparation and application of the terpenoid. In the invention, a carbon-drop diterpene new compound separated from leonurus is carbon-drop labdane diterpene obtained from the nature for the first time. The compound can obviously shorten the PT (prothrombin time), APTT (activated partial thromboplastin time) and TT (thrombin time) in vitro and obviously increase the amount of FIB (fibrinogen) in blood, and realizes a certain effect on enhancing the coagulation function, thereby providing a new option for developing a novel natural coagulation drug.
WO2011020079A1 Antibodies against human respiratory syncytial virus (rsv) and methods of use Provided herein are antibodies or antigen-binding fragments thereof that immunospecifically bind to the fusion (F) protein of Respiratory Syncytial Virus (RSV). Also provided are methods for of prevention, treatment and diagnosis of viral infection and/or the treatment of one more symptoms of RSV-mediated disease. Methods of generating antibodies that immunospecifically bind RSV F protein also are provided.
WO2007054309A2 Use of clodronic acid for the treatment of navicular syndrome The invention relates to the use of clodronic acid, the addition salts or esters thereof as an active substance for producing a medicament that is utilized for the treatment of navicular syndrome with an osteoporotic component in horses.
US20080140138 Inhibition of inflammatory cytokine production by stimulation of brain muscarinic receptors Methods for inhibiting pro-inflammatory cytokine release or inflammation in a vertebrate are provided. The methods comprise activating a brain muscarinic receptor of the vertebrate, or directly stimulating a vagus nerve pathway in the brain of the vertebrate. Also provided are methods for conditioning a vertebrate to inhibit the release of a pro-inflammatory cytokine or reduce inflammation in the vertebrate upon experiencing a sensory stimulus. The methods comprise (a) activating a muscarinic brain receptor or directly stimulating the vagus nerve pathway in the brain of the vertebrate and providing the sensory stimulus to the vertebrate within a time period sufficient to create an association between the stimulus and the activation of the brain muscarinic receptor; and (b) repeating step (a) at sufficient time intervals and duration to reinforce the association sufficiently for the inflammation to be reduced by the sensory stimulus alone.
US20080261898 Composition and method for cancer treatment and prevention Compounds, compositions, methods and kits are provided for treating, reducing the risk of, or preventing diseases and/or conditions, such as diseases associated with angiogenesis and/or abnormal cell proliferation, such as cancer. Compounds of the present invention have antiangiogenic and anti-cancer activity with minimum toxic effects on normal cells. Methods for preparing and manufacturing the compounds and pharmaceutical compositions are also provided.
WO2007135410A1 Ruthenium ii compounds A ruthenium (II) compound of formula (I), or a solvate form thereof for use in a method of therapy, wherein: R1 R2 R3 R4 R5 and R6 are independently selected from H, C1-7alkyl, C5-20aryl, C3-20heterocyclyl, halo, ester, amido, acyl, sulfo, sulfonamido, ether, thioether, azo and amino, or R1 and R2 together with the ring to which they are attached form a saturated or unsaturated carbocyclic or heterocyclic group containing up to three 3- to 8- membered carbocyclic or heterocyclic rings, wherein each carbocyclic or heterocyclic ring may be fused to one or more other carbocyclic or heterocyclic rings; X is halo or a neutral or negatively charged O, N- or S- donor ligand; m is -1, 0, 1 or 2; q is 1, 2 or 3; RC1 and RC2 independently represent one or more optional substituents selected from hydroxy, C1-7 alkoxy, C5-20 aryloxy, C1-7 alkyl, carboxy, C1-7 alkyl ester and C5-20 aryl ester; RN1 and RN2 are independently selected from hydroxy, C1-7 alkoxy, C5-20 aryloxy, C1-7 alkyl, carboxy, C1-7 alkyl ester and C5-20 aryl ester; or RN1 and RN2 together with the pyridine rings to which they are bound form an tricyclic heteraromatic moiety, where the ring formed by RN1 and RN2 together may be optionally substituted by one or more substituents represented by RC3 selected from: hydroxy, C1-7 alkoxy, C5-20 aryloxy, C1-7 alkyl, carboxy, C1-7 alkyl ester and C5-20 aryl ester.
CN103385884A Application of gastrodin to preparing medicaments for preventing and treating Alzheimer's disease The invention discloses an application of gastrodin to preparing medicaments for preventing and treating Alzheimer's disease. Alzheimer's disease (AD) is a neurodegenerative disease, and pathological characteristics comprise neuro fibrillary tangles formed in cells, hyperplasia of reactive microglia and glial cell, and the like, wherein the extracellular deposition of amyloid A beta is the main pathogenetic reason of AD. An AD small mouse taking a gastrodin-containing fodder is substantially improved in spatial-memory learning ability, substantially reduced in A beta level in brain and serum, and substantially reduced in amyloid plaques and microglia in brain tissue, and thus it is indicated that gastrodin is capable of preventing A beta deposition and decreasing active components causing AD mouse brain gastrodin.
US20120100204 TGF-Beta Stimulating Agent Compositions and Combinations Compositions and methods for preventing, inhibiting or treating a disorder associated with the loss of normal adult tissue architecture are provided.
US20050069583 Solid, digestable mixture of alginate, (bi)carbonate and polyol; gastrointestinal disorders A solid, ingestible composition comprising: a. an alginate; b. a bicarbonate and/or carbonate; and c. a C2-C5 polyol or poly(C2-C5 alkylene glycol).
CN101961339A Application of 23-HBA for preparing drug to reduce cardiotoxicity caused by adriamycin The invention relates to the field of natural drugs, in particular to the application of 23-hydroxybetulinic acid (23-HBA) for preparing a drug to reduce cardiotoxicity caused by adriamycin. When being combined with adriamycin, the 23-hydroxybetulinic acid can reduce the consistency of the adriamycin in heart tissues of tumor mice, reverse eardiotoxieity caused by the adriamycin and improve cardiac function, thereby being capable of being used as a myocardial protecting agent of the adriamycin as an antitumor drug.
WO2009091476A1 Compositions and methods for treating cancers This invention provides a combination of ATP-competitive BCR-ABL inhibitor and a non-ATP competitive BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with BCR-ABL.
WO2011081221A1 Therapeutic agent (y - 39983 ) for corneal endothelial dysfunction The present invention aims to provide a means for effectively and conveniently treating diseases wherein corneal endothelial cells poor in proliferative capacity in vivo are damaged. The present invention provides a therapeutic agent for corneal endothelial dysfunction containing (R) - ( + ) -N- (lH-pyrrolo [2, 3 -b] pyridin-4-yl) -4- (1 -aminoethyl) benzamide or a pharmacologically acceptable salt thereof (compound (Ia) ) as active ingredient, an agent for promoting adhesion of corneal endothelial cells, containing compound (Ia), a culture medium for corneal endothelial cells, containing the agent for promoting adhesion, an implant for corneal endothelial keratoplasty, containing corneal endothelial cells, scaffold and compound (Ia), and a production method of a corneal endothelial preparation, including a step of cultivating corneal endothelial cells using the culture medium.
US7211587 Administering compounds such as N-{3-Chloro-4-[(6,7-dimethoxy-4-quinolyl)-oxy]phenyl}-N'-(3-isoxazolyl)urea for therapy of malignant tumors An object of the present invention is to provide compounds having potent antitumor activity. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein X and Z represent CH or N; Y represents O or S; R1, R2, and R3 represent H, alkoxy or the like; R4 represents H; R5, R6, R7, and R8 represent H, halogen, alkoxy or the like; R9 and R10 represent H, alkyl or the like; and R11 represents optionally substituted azolyl.
WO2010136449A1 Akg composition and use thereof in the production of a drug The present invention relates to a composition of 1-O-alkylglycerol (AKG), characterised in that said composition comprises (in wt %): - at least 85% of a combination of AKG in C18:1 n-9 and C16:1; - less than 0.5% of AKG in C18:0; - less than 15% of AKG in C12:0 and C14:0. The invention also relates to the use of such a composition for the production of a drug for treating cancer.
CN102846673A Composition for improving human sperm motility and quality The invention discloses a composition for improving human sperm motility and quality, which comprises zinc, selenium, vitamin E, folic acid, vitamin B12, vitamin C, fructose, and citric acid. The composition of the invention is safe and effective for long-term administration, and has significant safety.
US7572817 Carboxypeptidase U inhibitors; thrombosis, atherosclerosis, adhesions, dermal scarring, cancer, fibrotic conditions, inflammatory diseases; e.g. 2-[(6-Aminopyridin-3-yl)methyl]-3-mercapto-5-[3-(pyrrolidin-1-ylcarbonyl)phenyl]pentanoic acid The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.
EP1203583B1 Remedies for arthrosis deformans An additional novel pharmacological effect of useful mercaptoacylcysteine derivatives. Remedies for arthrosis deformans comprising compounds represented by general formula [I] or salts thereof as the active ingredient. In formula [I], A represents lower alkylene exemplified by linear or branched C1-6 alkylene such as methylene, ethylene, (dimethyl)methylene and (diethyl)methylene.
WO2014096212A1 NOVEL TRICYCLIC 3,4-DIHYDRO-2H-PYRIDO[1,2-α]PYRAZINE-1,6-DIONE DERIVATIVES AS GAMMA SECRETASE MODULATORS The present invention is concerned with novel tricyclic 3,4-dihydro-2H-pyrido[l,2-a]pyrazine-l,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, L, Y, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament for the treatment of i.a. Alzheimer's disease.
WO2005009473A1 Antifungal aerosol external preparation Antifungal aerosol external preparations that are improved with respect to properties, such as skin penetration of antifungal ingredients, and do not cause corrosion of aerosol can. In particular, antifungal aerosol external preparations comprising a raw liquid, the raw liquid composed of a mixture of an antifungal ingredient, water and an HLB 1 to 9 lipophilic surfactant, and an alcohol.
WO2008137081A1 Substituted ( 5, 6 ) -dihydronaphraalenyl compounds as reversible male contraceptives The invention provides a method for inhibiting spermatogenesis in a mammal, as well as a reversible contraceptive for use in a mammal.
US8742103 Separation of triazine derivatives enantiomers using tartaric acid The present invention relates to a new process of separation of triazine derivatives enantiomers involving tartaric acid.
CN102973512A Adriamycin-loaded albumin nano-particle preparation with folate receptor targeting function and preparation method thereof The invention belongs to the technical field of medicines, and in particular relates to an adriamycin-loaded albumin nano-particle preparation with folate receptor targeting function and a preparation method thereof. The preparation method comprises the following steps of simultaneously connecting dextran-folate and dextran to albumin through a Maillard reaction to obtain an albumin-detran-folate compound; mixing adriamycin and water liquid of albumin-detran-folate covalent compound in an acidic condition, regulating the pH value of the liquid, and heating to prepare the stable adriamycin/albumin-detran-folate nano-particle with folate receptor targeting function. According to the adriamycin-loaded albumin nano-particle, the embedding amount and embedding efficiency of adriamycin can respectively reach 14 percent and over 90 percent; dynamic light scattering results indicate that the hydrated radius of the nano-particle is between 14 and 100nm and kept stable for a long time; and transmission electron microscope results indicate that the nano-particle with a sphere-similar appearance has better dispersibility. The nano-particle can be widely applied to the field of targeting medicine delivery.
CN101317942B Bone-setting alcohol The invention discloses osteopathic liquor used for treating fraction reduction and soft tissue injuries. The liquor is made from the raw materials with the following weight portions: 10 to 20 portions of angelica sinensis, 10 to 20 portions of red peony root, 10 to 20 portions of white peony root, 10 to 20 portions of Szechwan Lovage Rhizome, 13 to 23 portions of peach seed, 10 to 20 portions ofsafflower, 13 to 23 portions of india madder root, 10 to 20 portions of rhubarb, 10 to 20 portions of manyleaf paris rhizome, 10 to 20 portions of gardenia, 10 to 20 portions of frankincense, 10 to 20 portions of Myrrhe and 2100 to 2900 portions of white spirit. During the preparation, the raw material drugs are put in a vessel which is filled with white spirit to be immersed for 15 days. Then, after the residue filtering, the osteopathic liquor is obtained. The orthopedic liquor is provided with obvious effects. With the outer applying method directly acting on the affected part, fast and strong detumescence analgesic effect is provided. Especially for the fraction reduction, the blood stasis dispersing and analgesic effect is more miraculous after the reheating. Pains of patients can berelieved rapidly. Anesthetic action is substituted, no side-effect is provided, and the liquor can be called perfect osteopathic liquor.
WO2007115997A3 Combination preparations from modafinil, ritalin and topiramat for use in cocaine dependency and/or for treating impulse control disorders The invention relates to combination preparations from Modafinil, Ritalin and Topiramat and/or the derivatives thereof for use in the withdrawal and/or substitution therapy of cocaine dependency and/or for treating impulse control disorders.
US20090149416 2' and 3'-Substituted Cyclobutyl Nucleoside Analogs for the Treatment Viral Infections and Abnormal Cellular Proliferation Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.
WO2012169200A1 Sema5b peptides and vaccines including the same As discussed in detail herein, isolated epitope peptides derived from SEMA5B bind to an HLA antigen and induce cytotoxic T lymphocytes (CTL) and thus are suitable for use in the context of cancer immunotherapy, more particularly cancer vaccines. The inventive peptides encompass both the above mentioned amino acid sequences and modified versions thereof, in which one, two, or several amino acids are substituted, deleted, inserted or added, provided such modified versions retain the requisite HLA binding and/or CTL inducibility of the original sequences. Further provided are polynucleotides encoding any of the aforementioned peptides as well as pharmaceutical agents or compositions that include any of the aforementioned peptides or polynucleotides. The peptides, polynucleotides, pharmaceutical agents or compositions of this invention find particular utility in the treatment and/or prevention of cancers and tumors, including, for example, esophageal cancer, NSCLC, RCC and SCLC.
US20120184528 7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
EP2549877A1 Composition and method for preventing oral disease A composition and method of stabilized chlorine dioxide at a concentration range of about 0.005% to about 0.800% (w/v) at a pH in the range of 6.0 to 7.4 for the prevention of oral diseases caused by dental biofilm and plaque accumulation, such as gingivitis and periodontitis, through bactericidal properties is disclosed. The bactericidal properties of stabilized chlorine dioxide are further expanded to include reduction (kill) of anaerobic/aerobic/facultative gram-negative and gram-positive oral bacteria occurring in plaque or polymicrobial biofilms. The composition may be in the form of wash, rinse, soak, paste, gel, aerosol spray, or other suitable delivery system.
CN103012778A Water-soluble taxol polymer with tumor actively-targeted property The invention discloses a water-soluble polymer containing taxol and taxol ester and actively targeting a tumor and a preparation method of the polymer. The water-soluble polymer is prepared by conjugating a polymer containing taxol or docetaxel with polyglutamic acid, and tumor actively-targeted molecular folic acid is modified on the structure basis of polyglutamic acid-taxane compounds. The water-soluble polymer disclosed by the invention can be used for treatment of tumors.
WO2011064303A1 Sialochimeric compounds The present invention discloses a new class of compounds that exhibit an inhibitory effect on influenza virus type A and B, which may or may not be resistant to other drugs, as well as on other types of viruses, such as flavivirus but also on protozoa and other micro-organisms, their preparation methods, pharmaceutical formulations containing them and their use as medicinal products for the treatment of various conditions caused by particular microorganisms, including viruses, bacteria and protozoa, which affect animal and human health.
CN1915387A Medicinal food for treating disease of night sweat in type of the sinking of qi, and preparation method A medical food for treating night sweating is prepared from ginseng, tuckahoe, non-glutinous round-grained rice and edible salt. Its preparing process is also disclosed.
WO2010105110A1 Pharmaceutical combinations comprising rdea119/bay 869766 for the treatment of specific cancers The present invention relates to the field of oncology and provides compositions and methods for treating specific cancers, including non small cell lung cancer, breast cancer, thyroid cancer, pancreatic cancer, colon cancer, melanoma, hepatoma and adenocarcinoma. Particularly, compositions and methods involving administration, either simultaneously or sequentially, of pharmaceutical combinations comprising (S)-N- (3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-l-(2,3- dihydroxypropyl)cyclopropane-l -sulfonamide with other compounds, to patients suffering from cancer are described.
CN101716243A Qingkailing gelling agent for eyes and preparation method thereof The invention relates to a qingkailing gelling agent for eyes and a preparation method thereof. The invention provides a local medicine for treating the inflammatory eye diseases such as the conjunctivitis, the keratitis, the iritis, the endophthalmitis and the like. The used auxiliary materials comprise a gel substrate, an osmotic pressure regulator, a bacteriostatic agent, a pH regulator and the like. In the invention, the medicament form of the medicine of qingkailing is enriched by optimizing the auxiliary materials and improving the process, a mode of local administration is adopted, as a result, the medicine directly reaches an acting position, the effective medicine concentration in eyes is increased, the administration dose is small, sothe adverse reaction caused by venous administration is effectively avoided.
CN103381197A Externally applied liniment used for treating alopecia seborrhoeica The invention provides an externally applied liniment used for treating alopecia seborrhoeica. Severe epilation due to pathological causes poses great harm to the appearance of people, is a heavy blow to the confidence of people and influences career choices, marriage and even the future of people. The liniment provided by the invention comprises 3 g of salicylic acid, 3 g of resorcinol, 0.25 g of menthol, 5 ml of a coal tar solution and 100 ml of alcohol with mass percentage concentration of 5%. The above-mentioned components are fully mixed to obtain the liniment. The liniment is used for treating alopecia.
US20110160213 Pharmaceutical compositions for the treatment of inflammatory and allergic disorders The present invention relates to the pharmaceutical compositions, more particularly to the pharmaceutical compositions comprising novel phosphodiesterase type 4 (PDE4) inhibitors, and their use in treating allergic and inflammatory disorders.
US7087613 Treating abnormal cell growth with a stable polymorph of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride A method of monotherapy for a subject suffering from abnormal cell growth expressing the epidermal growth factor receptor (EGFR) which comprises orally administering to the subject a therapeutically effective amount of a crystalline polymorph of the hydrochloride salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine so as to treat the subject.
US8779141 Viral inhibitors The present invention relates to imidazo[4,5-c]pyridine compounds and pharmaceutical compositions for the treatment or prevention of viral infections, wherein the imidazo[4,5-c]pyridine compounds have the formula:
US20090076098 Methods, kits, and compounds for determining responsiveness to treatment of a pathological disorder by epothilones The invention provides methods, kits and compounds for determining the potential responsiveness of a subject suffering from a pathological disorder, including non-small cell lung cancer (NSCLC), to treatment with an epothilone by analyzing the gene expression profile and/or certain molecular markers in a sample obtained from said subject. The invention further relates to methods, compounds and uses of said compounds for treating subjects suffering from said pathologic disorder, optionally in combination with other therapeutic agents. Also provided are genes and/or proteins encoded by them whose expression level have been determined to differ between epothilone responders and epothilone non-responders.
US7678549 Polyphenol inhibition of nucleoside diphosphate kinase-B activity and cancer metastasis Aggressive human tumor cells from disparate tissues were found to secrete nucleoside diphosphate kinase-B (NDPK-B) as a phosphoprotein into the extracellular environment. The secreted enzyme was capable of trasphosphorylation activity in the absence of a phosphoryl donor, thereby producing elevated level of extracellular ATP that plays a significant role in angiogenesis required for the growth of cancer cells and cancer metastasis. A series of structurally related non-nucleotide anticancer compounds such as ellagic acid (EA), epigallocatechin gallate (EGCG), and epicatechin gallate (ECG) were found to inhibit the activity of secreted nucleoside diphosphate kinase-B as well as angiogenesis. The nucleoside diphosphate kinase-B inhibition data disclosed herein can be used in predicative models to design novel inhibitors of nucleoside diphosphate kinase-B activity.
CN101428050A Active composition for treating thrombus, cardio-cerebrovascular system diseases The invention relates to an active composition used for curing thrombus and cardiovascular and cerebrovascular diseases, in particular to an active composition contained with ginsenoside Rg1 and ginsenoside Rb1 and obtained by extracting and separating the notoginseng of araliaceae panax plants. The active composition is formed by combining panoxatriol ginsenoside and panaxadiol ginsenoside and comprises 80 to 99 percent of the panoxatriol ginsenoside and 1 to 20 percent of the panaxadiol ginsenoside according to the mass percent. The scientific research shows that the composition of the ginsenoside Rg1 and the ginsenoside Rb1 can improve the haemodynamics and the blood quality, prevent the blood vessel and the neural inflammation and has good therapeutic effect on the thrombus and the cardiovascular and cerebrovascular diseases.
CN102552328A Preparation method of compound fish oil nano-emulsion The invention discloses a preparation method of a compound fish oil nano-emulsion. The preparation method is characterized by comprising the following steps of: heating 10-20 parts of emulsifying agent by weight and adding 10-20 parts of auxiliary emulsifying agent by weight; agitating uniformly; adding 3-6 parts of antioxidant by weight and agitating uniformly to form faint yellow and uniform liquid for future use; marking the liquid as X liquid; uniformly mixing 4-8 parts of fish oil by weight and 6-12 parts of salad oil by weight; adding the X liquid and agitating uniformly; dissolving a water-soluble vitamin with 15-30 parts of water by weight and agitating uniformly; and then, adding the mixed solution into the X liquid and agitating while adding the solution; and finally, homogenizing and emulsifying the final solution by a colloid mill to obtain the compound fish oil nano-emulsion, wherein the water-soluble vitamin is selected from at least two of vitamin C, taurine and folic acid. According to the nano-emulsion disclosed by the invention, the emulsifying agent, the auxiliary emulsifying agent and the antioxidant are added, so that the fish oil can be better covered to carry out the preparation of the fish oil nano-emulsion; and the fish oil nano-emulsion can be compounded with other materials so that the fish oil nano-emulsion can be added into cakes, yoghourt and ice creams.
US6916838 1-benzylpyrazole-3-carboxylic acid tricyclic derivatives as cannabinoid receptor antagonists Tricyclic derivatives of 1-benzylpyrazole-3-carboxylic acid which are antagonists of the cannabinoid CB2 receptors; their method of preparation and pharmaceutical compositions containing them.
US20120196846 Anti-rsv compounds The present invention relates to anti-RSV compounds of Formula (I) and methods for use of the compounds in the treatment and prevention of RSV infection.
WO2007141533A2 Fkbp-l and uses thereof Disclosed are methods and compositions that employ FKBP-L polypeptides for modulating angiogenesis and/or tumor metastasis. The FKBP-L polypeptides may be used for the treatment of disorders mediated by angiogenesis such as cancer.
DE102006062433A1 Deodorant or antiperspirant composition comprises a deodorant or antiperspirant agent and taurine in a carrier Deodorant or antiperspirant composition comprises a deodorant or antiperspirant agent and taurine in a carrier.
CN102895648A Clinical nutrition emulsion and preparation method thereof The invention, belonging to the technical field of clinical medicine, particularly relates to a clinical nutrition emulsion and a preparation method thereof. The clinical nutrition emulsion disclosed herein has the advantages of safety, reliability, and good stability. The clinical nutrition emulsion disclosed herein comprises 200-300g of lactalbumin hydrolysate, 200-300g of refined white granulated sugar, 200-300g of maltodextrin, 80-100g of medium-chain triglyceride, 90-100g of peanut oil, 10-15g of compound emulsifier, 5-15g of composite minerals, 0.5-1.5g of multivitamin, 30-50g of compound stabilizer, and 1-3g of immuno-potentiating active material. The preparation method disclosed herein comprises the following steps: respectively dissolving the raw materials and auxiliary materials in oil phase and water phase, mixing after dissolving completely; adding a colloid mill to the mixed solution, then carrying out homogenization on the formed colloid; after the colloid is homogeneous, bottling, sealing and sterilizing, wherein the sterilization temperature is 100-150 DEG C, and the sterilization time is 10-25 min; and finally labeling, and inspecting to obtain finished products.
US20090074716 method for treating influenza virus infection The invention concerns the treatment of orthomyxovirus infections with inhibitors of the ubiquitin protease system, in particular proteasome inhibitors.
CA2635787A1 Cycloalkanecarboxamide derivative and method for producing same Disclosed is a novel cycloalkanecarboxamide derivative having a selective cathepsin K inhibitory activity. Also disclosed is a method for producing such a cycloalkanecarboxamide derivative. Specifically disclosed is a cycloalkanecarboxamide derivative represented by the general formula (I) below or a pharmaceutically acceptable salt thereof. (I) (In the formula, R1 and R2 respectively represent a (substituted) alkyl group, a (substituted) alkenyl group, a (substituted) alkynyl group, a (substituted) aromatic hydrocarbon group, a (substituted) heterocyclic group; ring A represents an alkylidene group having 5-7 carbon atoms; and B represents a formyl group or a hydroxymethyl group.)
WO2013066179A1 Liposomal corticosteroids for treatment of inflammatory disorders in humans The invention relates to a pharmaceutical composition comprising liposomes composed of non-charged vesicle-forming lipids, optionally including not more than 10 mole percent of negatively charged vesicle- forming lipids and/or not more than 10 mole percent of PEGylated lipids, the liposomes having a selected mean particle diameter in the size range of 40-200 nm and comprising a first corticosteroid in water soluble form, for the site-specific treatment of inflammatory disorders in humans, providing in human patients a fast, strong, and durable anti-inflammatory effect for at least 2 weeks at a dose of at most 5 mg/kg body weight of prednisolone or an equipotent dose corticosteroid other than prednisolone at a treatment frequency of at most once per two weeks. Furthermore the present invention relates to the application of the above-mentioned pharmaceutical composition given as intervention therapy in inflammatory disorders such as rheumatic disease or a related inflammatory connective tissue disorder, inflammatory diseases of the kidney or inflammatory bowel disorders, in combination with chronic therapy with a second free corticosteroid formulation or in combination with chronic treatment with a disease- modifying agent such as methotrexate.
CA2304568C Olanzapine pamoate formulations The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.
US20090054363 Genetic markers and methods for detecting and treating cancers The present invention provides genetic markers, SOX5 and SPARC, for distant metastasis and poor prognosis of detection of the high risk potential for cancer patients. In addition, the present invention also provides a method to predict the risk potential for cancer patients with distant metastasis and poor prognosis. This method comprises obtaining a tissue sample from a patient, evaluating the expression levels of the SOX5 and/or SPARC genetic markers in the sample; and comparing the expression levels of genetic markers with those of non-cancerous tissues. The patient is determined to have the high risk of distant metastasis or poor prognosis when the expression level of SOX5 is higher, or when the expression level of SPARC is lower, than that of non-cancerous tissue. Furthermore, the identified genetic marker SOX5 and/or SPARC can also be used for cancer targeted therapy, because down regulation of SOX5 and/or up regulation of SPARC expression in NOD-SCID can retard tumor growth and inhibit cell proliferation, migration, invasion and metastasis.
WO2011069871A1 A method for providing emergency contraception using ulipristal acetate The invention provides a method for providing emergency contraception in a female subject, comprising providing the subject with a therapeutically effective amount of ulipristal acetate in an oral dosage form before, during or after a meal. The invention further provides a kit comprising i) an oral dosage form comprising ulipristal acetate and ii) a printed matter stating that ulipristal acetate may be taken with or without food.
US20090306191 Treatment of a disease or a condition associated with aberrant gene hypomethylation by a method involving tailored epigenomic modification Disclosed herein is a method for treating a subject having or suspected of having a disease or condition associated with aberrant hypomethylation of one or more genes in the subject, the method involving a tailored epigenomic modification of the subject using methylated polynucleotides directed to hypomethylated genes in the subject. Also disclosed herein is a medicinal composition for treating a subject having or suspected of having a disease or condition associated with aberrant hypomethylation of one or more genes in the subject, the composition including methylated polynucleotides directed to hypomethylated genes in the subject, so as to result in a tailored epigenomic modification of the subject upon administration.
US20130041013 Isoform of bruton's tyrosine kinase (btk) protein The use of compounds is described which are capable of functionally blocking at least one of the genes chosen from the group composed of EphA1, EphA2, EphA8, EphB2, CSF1R, VEGFR2, RAMP2, RAMP3, CLRN1, MAPK4, PIK3C2A, PIK3CG, GSK3alpha, GSK3beta, IRAK3, DAPK1, JAK1, PIM1, TRB3, BTG1, LATS1, LIMK2, MYLK, PAK1, PAK2, CDC2, BTK, PNRC2, NCOA4, NR2C1, TPR, RBBP8, TRPC7, FXYD1, ERNI, PRSS16, RPS3, CCL23 and SERPINE1, for the manufacture of a medicament destined to diminish the resistance to chemotherapeutic drugs in the therapeutic treatment of epithelial tumour pathologies. Also described is a method for the determination of the drug resistance in tumour cells, as well as a method for the identification of tumour stem cells.
WO2012092471A2 Novel tubulin inhibitors and methods of using the same Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof: R2-Y-Z-Q-A-R1 Formula (I) wherein R1, R2, Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.
WO2011112859A2 Methods relating to olanzapine pharmacogenetics There is significant variability in subject clearance, half-life and side-effects from treatment with olanzapine (OLZ) in subjects. Methods for aiding in determining therapeutic efficacy of olanzapine in a subject are provided according to embodiments of the present invention which include identifying in a subject sample whether UDP- glucuronosyltransferase 2B10 (UGT2B10) and/or UDP-glucuronosyltransferase 1A4 (UGT1A4) is "wild-type" or a variant associated with altered glucuronidation of an olanzapine metabolite compared to wild-type.
CN101225087A Coumarether compound and use of its composition The invention discloses a coumaric grass ethers extracted from compositae plants, or a salt or an ester accepted in pharmacy, or the application of the plant extracts of the compound for the preparation of medicine for curing autoimmune liver disease and viral hepatitis. As shown by the vitro and vivo experiments to the animal body, the coumaric grass ethers extracted from compositae plants, or a salt or an ester accepted in pharmacy has the advantages of effective therapy and improvement of the symptoms of autoimmune liver disease and viral hepatitis.
CN101384578A Radioligands for the 5 -ht1b receptor The present invention provides novel radioligands for the 5-HT1B receptor of the formula I.
EP1267886B1 Vitamin d compounds for the treatment of chronic allograft nephropathy in kidney transplant patients A method of stabilizing kidney function in transplant patients is disclosed. In one embodiment, the method comprises the steps of kidney transplant patient, wherein the transplant patient is undergoing immunosuppressive therapy, with a sufficient amount of vitamin D compound whereby the kidney function stabilizes.
US7799827 zearalenone-like macrolides, used to to inhibit nuclear factor kappa-beta (NF- kappa B) activation, as sucnscreen agents and in the treatment of inflammatory or autoimmune disorders and disorders involving malignancy or increased angiogenesis The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, X, Y, Z, and n are as defined herein.
WO2007120925A3 Crystal forms of o-desmethylvenlafaxine Methods for preparing crystalline forms of O-desmethylvenlafaxine a described.
US7060470 Isoflavone-β-D-glucan produced by Agaricus blazei in the submerged liquid culture and method of producing same The present invention relates to low and medium molecular weight isoflavone-β-D-glucan produced by submerged liquid culture of Agaricus blazei, a method of producing the isoflavone-β-D-glucan using autolysis enzyme of Agaricus blazei mycelia, and use of the isoflavone-β-D-glucan for anti-cancer and immunoenhancing effect.
US6969508 Buccal aerosol sprays or capsules using polar and non-polar solvent which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.
WO2010113179A3 Process for purifying eslicarbazepine acetate A process for purifying eslicarbazepine acetate is provided The crystalline particles of eslicarbazepine acetate having a median particle size between 5 μm and 20 μm and a specific surface area of from 0.1 m2/g to 10 m2/g as measured by B.E.T. method are obtained Eslicarbazepine acetate having purity greater than 99.0% as measured by high performance liquid chromatography and a pharmaceutical composition containing the same are also provided.
WO2012019288A1 Foamable compositions of stabilized chlorite The present application relates to foamable compositions and foams comprising stabilized chlorite, including stabilized chlorite solutions such as OxovasinTM, and to medical uses thereof, in particular for wound healing. The foamable compositions comprise at least one foaming agent, stabilized chlorite, water and optionally, a buffering agent.
WO2014156505A1 Jelly-like tablet and jelly-like lozenge using same [Problem] The purpose of the present invention is to provide a jelly-like tablet and a jelly-like lozenge using that jelly-like tablet that suppress adherence on teeth and for which water separation is difficult. [Solution] Carrageenan is mixed with agar, and moisture content is set at 30% by weight or less to be able to control adherence to teeth and provide a superior dosing sensitivity while being able to suppress water separation of the jelly-like tablet.
CN103040791A Asiatic acid lipid nanoparticle capable of stimulating oral absorption and preparation method thereof The invention discloses an asiatic acid lipid nanoparticle capable of stimulating oral absorption and a preparation method thereof. The asiatic acid lipid nanoparticle is prepared by taking a lipid material as a carrier and asiatic acid as a main drug through a solvent diffusion method. The particle size of the obtained lipid nanoparticle is smaller than 700nm, the entrapment rate is 40-90% and the drug-loading rate is 7-11%. By utilizing the nanoparticle, the intestinal drug absorption can be increased, and the oral bioavailability is improved.
US20120039909 Epigenetic mechanisms re-establish access to long-term memory after neuronal loss The invention relates to methods and products for enhancing and improving recovery of lost memories. In particular the methods are accomplished through the increase of histone acetylation.
WO2009143507A3 Silent desensitizers of neuronal nachr and methods of use thereof One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor.
US20070003610 Application of lipid vehicles and use for drug delivery The present invention relates to compositions and methods for the administration of lipid-based vehicles to treat various disorders, including bladder inflammation, infection, dysfunction, and cancer. In various aspects, the compositions and methods of the invention are useful for prolonged delivery of drugs, e.g., antibiotics, pain treatments, and anticancer agents, to the bladder, genitourinary tract, gastrointestinal system, pulmonary system, and other organs or body systems. In particular, the present invention relates to liposome-based delivery of vanilloid compounds, such as resiniferatoxin, capsaicin, or tinyatoxin, and toxins, such as botulinum toxin, for the treatment of bladder conditions, including pain, inflammation, incontinence, and voiding dysfunction. Further related are methods of using these vehicles alone or in conjunction with antibodies, e.g., uroplakin antibodies, to improve duration of liposome attachment, and provide a long-term intravesical drug delivery platform. The present invention specifically relates to antibody-coated liposomes that are useful for targeting specific receptors for drug, peptide, polypeptide, or nucleic acid delivery. In one particular aspect, the present invention relates to liposomes coated with antibodies against nerve growth factor (NGF) receptor and containing NGF antisense nucleic acids, which are used as a treatment for neurogenic bladder dysfunction.
US20110039829 Pyrazole-carboxamide derivatives as p2y12 antagonists The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
US20100120711 Ampk potentiator containing chito-oligosaccharide Disclosed herein is a composition for promoting AMPK activity, which comprises a chito-oligosaccharide as an active ingredient. The present composition affects the enzymes related to AMPK and lipid metabolism, and thus helps recovery from the condition lacking energy by various functions of controlling metabolism. Therefore, the present composition can enhance energy metabolism, thus making the composition effective for improving exercise capacity and reducing fatigue. The present composition can be used in the preparation of food or medicinal product as an endurance builder or for the prevention and improvement of fatigue.
US20100168685 Serially Dispensable Antiseptic Wet Wipes Moistened with Tincture of Green Soap An apparatus and method of use are disclosed for rapidly and repeatedly cleaning a skin area during tattooing or body piercing. The apparatus includes a plurality of serially dispensable, antiseptic wet wipes pre-moistened with “tincture of green soap” solution. It eliminates any need to dilute a concentrated green soap solution or clean a spray bottle, and allows a tattoo artist to quickly and conveniently obtain and use a wet wipe of the invention in a controlled and consistent manner using only one hand, thereby avoiding interruption of the procedure and contamination of the wet wipe. The wet wipes and/or green soap can be medically approved, and the wipes can be disposable and/or made from non-woven paper, with a preferable size of 19.5 by 17.0 centimeters. The wet wipes can be interleaved or formed in a continuous sheet with perforated separations, and can be folded, or configured in a roll.
WO2008082839A2 Pim kinase inhibitors as cancer chemotherapeutics Thieno[3,2-d]pyrimidiii-4-one derivatives as inhibitors of Pim kinases, ways to make them and methods of treating patients using them are disclosed.
CN101313969A Spraying agent for stubborn psoriasis The invention relates to stubborn dermatitis spray, which is characterized in that: Japanese dock root, long-nosed pit viper, bigfruit elm fruit, Chinese prickly ash, cyrtomium rhizome, common cnidium fruit, periostracum cicadae, angelica dahurica, phellodendron, polistes mandarinus nest, Chinese lobelia, kuhseng, Chinese atractylodes, Chinese goldthread rhizome, colophony, liquorice and so on are taken for extracting concentrated solution, and the concentrated solution is uniformly mixed with centipede powder, realgar powder, camphor powder, alum powder and ketoconazole; and the stubborn dermatitis spray is prepared after irradiation sterilizing and canning.
CA2588495C The utility of uridine nucleosides in the treatment of cachexia Pyrimidine nucleotide precursors including acyl derivatives of cytidine, uridine, and orotate, and uridine phosphorylase inhibitors, and their use in enhancing resistance to sepsis or systemic inflammation are disclosed.
WO2014057511A1 Use of emicorons as selective inducers of damage to the telomere dna The hydrosoluble emicoron derivatives of the general formula (I) are particularly effective as inducers of selective telomere and non- telomere DNA damage in tumour and transformed cells. The damage is measured as the ability to cause a number of TIF foci in transformed cells that is equal to or higher than 4 at a 0.1 uM dose of the compound of the formula (I). Such emicoron derivatives can be used in a kit together with other known anti-tumour drugs, such as, for example, topoisomerase I inhibitors, for the combined, simultaneous, delayed or sequential administration. The emicoron compounds of the formula (I) are particularly useful in the therapy of tumours that do not express p53 protein or express an inactive p53 protein and of tumours that maintain telomeres by mechanisms different from telomere maintenance by telomerase, and in the removal of cancer stem cells. Also, the method for the preparation of emicoron compounds of the formula (I), which envisages the use of intermediates such as the Ν,Ν'-bis [2-(1-piperidino)-ethyl] - 1-(1-piperidinyl)-7- [3-(1-piperidino)- butynyl]-perylene-3,4;9,10-tetracarboxyl diimide, is described.
WO2014087165A1 Tankyrase inhibitors The present invention relates to a compound of formula I wherein X is C(R6) or N, Y is C or N, and ring A, ring B, R1 and R2 have the meanings defined herein, provided that when ring B is carbocyclic, X is C(R6); or a pharmaceutically acceptable salt or solvate thereof. The compounds are tankyrase-1 and tankyrase-2 inhibitors and are useful in the treatment of a number of conditions, including cancer.
US7157447 Useful for treating HIV infection and AIDS The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV
WO2009055937A1 Altered n-cadherin processing in tumor cells by furln and proproteln convertase 5a (pc5a) The present invention relates to a method for diagnosis and/or prognosis of cancer and for monitoring the progression of cancer and/or the therapeutic efficacy of an anti-cancer treatment in a subject by determining the molecular form of cadherin at the cell surface of cancer cells in the subject. The invention also relates to a method for preventing, inhibiting or treating cancer or its metastasis in a subject by increasing the adhesive forms of cadherin and/or decreasing the non-adhesive forms of cadherin at the cell surface. The invention also relates to a method step of determining the expression level of furin and proprotein convertase 5A (PC5A).
US8580780 6 substituted 2, 3,4,5 tetrahydro-1H-benzo[d]azepines as 5-HT2C receptor agonist The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R6 is —S—R14; and other substituents are as defined in the specification.
WO2008133129A1 Therapeutic agent for glaucoma comprising adenosine a2a receptor agonist as active ingredient GW-328267, UK-432097, or a compound represented by the general formula (1) or a salt thereof, which is an adenosine A2A receptor agonist, exhibits an excellent ocular hypotensive effect in the test on decrease in ocular tension, and is therefore useful as a prophylactic or therapeutic agent for glaucoma or ocular hypertension. In the general formula, W represents a hydrogen atom or a group represented by the general formula (8); the ring A represents a benzene ring, a pyridine ring, a pyrazole ring, an imidazole ring, a cyclohexane ring or the like; X represents a single bond, O-CH2-CH2, NH-NH=CH, NH-CH2-CH2, CO-NH-CH2 or the like; Y represents CH or N; Z represents CH2 or O; R1 represents a hydrogen atom, a halogen atom, an alkyl group, an alkylaminocarbonyl group or the like; R2 represents a hydroxyalkyl group, an alkylamino group, an alkylaminocarbonyl group, a triazolyl group or the like; and R3 represents a hydrogen atom, an alkyl group or the like.
CN101274067B Method of medical ointment for activating blood circulation, removing stasis, dredging channels and collaterals, releasing swelling and relieving pain The invention provides a method for preparing an ointment which has the functions of activating blood circulation to dissipate blood stasis, dredging meridian, detumescence and reliving pain. The formula of the ointment comprises doubleteeth pubescent angilica root, dahurian angelica root, notopterygium roots, Chinese angelica, buck grass, cortex eucommiae, clematis root, twotooth achyranthes root, fortune's rhizoma drynariae, malaytea scurfpea fruit, suberect spatholobus stem, rhizoma homalomenae, prepared kusnezoff monkshood root, tuberculate speranskia herb, nux vomica, radix dipsaci from Sichuan of China, safflowers, divaricate saposhnikovia root, scorpion, centipede, frankincense, myrrh, dragon's blood, borneol and camphor. After going through pulverizing, dosing, grinding, extracting by using water and spreading on special cloth according to computation, the ointment is obtained. Hundreds of cases clinically prove that the ointment of the invention has the advantages of strong penetrability and quick drug effects, capable of strengthening the bones and muscles, dispelling cold and removing dampness, activating blood circulation to dissipate blood stasis, detumescence and has obvious curative effect on periarthritis humeroscapularis, headache, tumescence and anaesthesia caused by cervical spondylosis as well as diseases caused by lumbar disc protrusion such as hucklebone neuralgia, waist-leg pain, lumbar muscle strain, ankylosing spondylitis, parenchyma contusion, ill-defined masses, breast lump, peritendinitis, rheumatalgia, etc..
US20080300251 Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
CN102525917A Nimodipine micelle injection and preparation method thereof The invention discloses a nimodipine micelle injection and a preparation method thereof. The nimodipine micelle injection is prepared by using active ingredients, i.e. nimodipine and phospholipid/bile salt. According to the nimodipine micelle injection disclosed by the invention, the solubility of the nimodipine is greatly increased, and no crystal precipitation exists when the nimodipine micelle injection is diluted; the biocompatibility of the phospholipid/bile salt is good, and organic solvents with great toxic side effects, such as ethyl alcohol, propylene glycol and the like, are not needed to for solubilizing so that the toxicity of the nimodipine micelle injection is lowered, the vascular stimulation is little, and the adverse reaction of the nimodipine micelle injection is reduced; and the nimodipine micelle injection can be directly used for intravenous injection and can also be used for instilling after the nimodipine micelle injection is diluted to various degrees, and thus, the clinical administration is greatly facilitated.
CN101492463B Imidazopyridine derivative containing dioxane-pyridine The invention belongs to the pharmaceutical technical field and specifically relates to imidazopyridine derivatives which are shown in general formula (I) and contain dioxide heterocyclic pyridine, pharmaceutically acceptable salts and isomers thereof, wherein, R<1>, R<2>, R<3> and n are defined as in the specification. The invention also relates to preparation methods of the compounds, drug compositions containing the compounds and the application of the compounds in preparing drugs for preventing and/or treating digestive ulcer.
CN102038724A Formula of baste for treating baldness and preparation method thereof The invention discloses a formula of baste for treating baldness, which consists of the following components in percentage by weight: 15 to 25 percent of sesame flower, 15 to 25 percent of cockscomb flower, 0.5 to 1 percent of camphor, and 55 to 65 percent of white spirit. A method for preparing the formula of the baste for treating the baldness comprises the following steps of: taking the sesame flower and the cockscomb flower, and cutting the cockscomb flower into small pieces; immersing 15 to 25 percent of sesame flower and 15 to 25 percent of cockscomb flower into 55 to 65 percent of white spirit according to weight percentage, and sealing; filtering to remove residues after 15to 20 days; and adding 0.5 to 1 percent of camphor into the spirit for dissolution. During use, the medicinal liquor is applied to a bald area for three times a day. The invention has the advantages that: the formula is simple; and the baste does not have any side effect on a human body or influence human health.
US20080227869 Substituted nitrobenzene derivatives as pharmaceutical and other uses thereof A method for the prophylaxis or treatment of analgesic, hemostatic, antipruritic, antiussive or antiasthmatic action including administrating an effective prophylaxis or treatment amount of at least one compound of Formula I as the active ingredient, pharmaceutical carrier and/or recipient, wherein, A is one, two or three nitro groups, at 1, 3, and/or 5 position on the benzene ring; R is one, two or three linear or branched C1-6 alkyl groups, at 2, 4 and/or 6 position on the benzene ring.
CN101401852A Chinese and western combined externally applied formulation for treating empyrosis The invention discloses an external preparation combining Chinese and Western medicines for treating burn and scald. The preparation comprises the components in weight portion: 1 portion of antibiotic or bacteriophage, 80 to 110 portions of distilled water and 20 to 40 portions of rhubarb extractive. The external preparation has the advantages of no need for performing isolation skin-grafting operation, short treatment period, high cure rate, uneasy infection, no scar and low cost, and no scar and chromatosis after healing the burn and the scald even if the burn and scald areas reach II degree-III degree below 40 percent.
CN102526170A Catechu extract composition for resisting tubercle bacillus, preparation method of catechu extract composition, pharmaceutical preparation containing catechu extract composition, and application of catechu extract composition The invention discloses a catechu extract composition for resisting tubercle bacillus, a preparation method of the catechu extract composition, a pharmaceutical preparation containing the catechu extract composition, and application of the catechu extract composition. The catechu extract composition contains a flavanoid compound of which the purity is more than 50%, and the flavanoid compound takes catechin and/or epicatechin as main components. The main structural formulas (I) and (II) of the flavanoid compound are shown in the specifications, wherein R1, R2, R3, R4 and R5 are respectively and independently selected from hydrogen, C1-C6 alkyl, beta-D-glucopyranesyl, SO3 or PO3. By adopting a chromatographic process for refining and purifying the catechu extract composition disclosed by the invention, the effective content is as high as 99.5%. The catechu extract composition and the pharmaceutical composition thereof have excellent effects on improving or treating pulmonary tuberculosis, treating ulcerative bone tuberculosis and AIDS (Acquired Immune Deficiency Syndrome) complicated by tuberculosis, treating drug resistant tuberculosis, and especially treating drug resistant tuberculosis and AIDS complicated by tuberculosis.
WO2007060240A3 Method for demonstrating presence or absence of markers (eef1a1 or mark3 )associated with the presence and/or the chemosensitivity of tumors The invention concerns a novel diagnostic method for detecting the presence or the absence of a tumor and/or its sensitivity to chemotherapies in a mammal, in particular in a human being, by detecting and/or quantifying the presence of a novel biological marker in a biological sample previously collected in said mammal: an eEF1A1 protein and/or a MARK3 protein. The absence of an eEF1A1 protein or antibodies directed against an eEF1A1 protein or a fragment comprising at least one epitope of said protein, or a low concentration compared to concentrations observed in healthy persons or patients suffering from cancers sensitive to chemotherapies is characteristic of the presence or a tumor a priori resistant to the usual chemotherapies (chemoresistant). The presence of a MARK3 protein or antibodies directed against a MARK3 protein or a fragment comprising at least one epitope of said protein is characteristic of the presence of a tumor.
WO2006118278A1 Temperature-sensitive liposome and temperature-sensitive drug release system Temperature-sensitive liposomes comprising a liposome membrane and, carried thereby, not only a polymeric compound having a thermosensitive responsive region and a hydrophobic region but also polyethylene glycol.
CN101433619B Tinctura for eliminating tinea and relieving itching The invention discloses a tincture against tinea and itching. More than fifteen kinds of medicaments such as cortex phellodendri, indigo, rhubarb, pericarpium zanthoxyli, clove, peach kernel, pomegranate bark, Chinese gall are reasonably mixed and then subjected to crushing, extraction and separation, preparation, filtering, measuring and product finishing to obtain the tincture against tinea and itching. The tincture against tinea and itching is a transparent external use liquid preparation which has the smell of beetle fart and is brown yellow, and has obvious effects of treating chronic skin diseases such as neurodermitis, psoriasis, chronic eczema, lichen, ringworm of the foot, intractable prurigo, verruca acuminata, skin hyperkeratosis.
CN103181921A Ampicillin and cloxacillin benzathine breast injectant composition and preparation method thereof The invention relates to a breast injectant composition comprising ampicillin and cloxacillin benzathine and a preparation method thereof. The breast injectant composition comprises a diluent and a suspending agent; and a vector is white viscous paste prepared by a specific process. The breast injectant composition has the advantages of simple preparation process, constant quality, stable content, easiness for infusion, soft matrix and the like. Compared with an injection, the breast injectant composition is a paste preparation so as to have the advantages of high bioavailability, low release speed, long acting time, capability of preventing and treating bacterial invasion after the breast injectant composition is filled into a milk chamber, and the like.
EP1248602B1 Use of retinoid receptor antagonists in the treatment of cartilage and bone pathologies The present invention relates to methods for treating cartilage and bone pathologies, including bone growth related diseases such as osteoarthritis, comprising administering therapeutically effective amounts of retinoid receptor antagonists.
WO2008084312A3 Micronised particles of low-dosage strength active agents for powder formulations for inhalation The invention relates to micronised particles of a low-dosage strength active ingredient to be used in dry powder formulations for inhalation and methods for preparing them. In particular the invention provides micronised particles of low-dosage strength active ingredients which can easily and homogenously disperse in a dry powder formulation to be administered by means of a dry powder inhaler device. The invention is also directed to the formulations thereof in the form of powders for inhalation.
WO2013024011A1 Indazole compounds, compositions and methods of use A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.
US20100331295 Modulators of lxr Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
CN103665046A Ruthenium complex as well as preparation method and application thereof The invention discloses a ruthenium complex containing a pyridine derivative as well as a preparation method and an application of the ruthenium complex. The structural formula of the complex is shown in the formula (I). The preparation method comprises the steps: grinding a reaction initiator trans-[RuCl4(SOR1R2)2][(SOR1R2)2H] into fine powder; stirring the initiator and ligand or performing ultrasonic oscillation in a reaction solvent, wherein the molar rate of the initiator to the ligand is 1:2-1:8 and the reaction temperature is 25-80 DEG C; or carrying out backflow; filtering precipitate formed after ultrasonic oscillation, and washing with acetone and diethyl ether; and drying by a silicon rubber dryer and keeping overnight. According to the preparation method of the ruthenium complex, the reaction time is short and the yield is high; and by using the prepared NA MI-A derivate, the anti-metastasis pesticide effect of Lewis experimental lung-cancer mice is significant, and the toxicity is low.
US20110237571 Phthalazine derivatives The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.
US6911457 Diabetes imaging probes The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.
CN1907264A Compound sulfonamide suspensoid and its preparing process Disclosed is a compound sulfonamide turbid agent which comprises the following constituents (by weight percent): sulfadiazine 8-12, sulfamethoxazole 4-8, sulfamethoxydiazine 2-6, trimethoprim 2-6, and medicinal auxiliary materials including acid-base scale modifier, suspension auxiliary agent, acidifying agent, anti-oxidant, stabilizer and purified water.
CN101780068B Application of jungermanniaceae D in preparing anti-tumor medicaments and anti-tumor multi-drug resistance reversing medicaments The present invention provides a new use of jungermanniaceae D, namely the application of the jungermanniaceae D in preparing anti-tumor medicaments and anti-tumor multi-drug resistance reversing medicaments. Research results show that the jungermanniaceae D can inhibit the expression of a gene alpha subtype of topoisomerase II, can selectively inhibit the activity of the topoisomerase II and has an obvious anti-tumor action, and simultaneously the compound can inhibit P-glycoprotein and shows good tumor multi-drug resistance reversing activity, so the jungermanniaceae D is a chemotherapy medicament which specially has a development prospect, and can serve as a main component for preparing anti-tumor oral preparations and injections, multi-drug resistance reversing oral preparations and injections and the like.
WO2005082865A1 Fused bicyclic pyrimidine derivative [PROBLEMS] To provide a compound useful as a preventive or a remedy for inflammatory diseases, allergic diseases, autoimmune diseases and the like in which CC chemokine receptor 4 (CCR4) participates. [MEANS FOR SOLVING PROBLEMS] It is found out that a fused bicyclic pyrimidine derivative having a piperidino or piperazino group, to the 4-position of which a saturated ring is attached, at the 2-position and a substituted amino group at the 4-position has a favorable activity as a CCR4 function-controlling agent. It is further found out that this derivative is particularly useful as a remedy for inflammatory diseases such as dermatitis.
WO2014096115A1 Ciclesonide for the treatment of airway disease in horses The invention relates to the field of medicine, in particular to the field of veterinary medicine. The invention relates to glucocorticoids, especially ciclesonide or a pharmaceutically acceptable derivative thereof, for the treatment of airway disease in horses, such as pulmonary disease, preferably recurrent airway obstruction (RAO), Summer Pasture Associated Obstructive Pulmonary disease (SPAOPD), and inflammatory airway disease (IAD).
US20110263695 NFAT Signal Inhibitor and Hair-Growing Agent An NFAT signal inhibitor and the like are provided. An NFAT signal inhibitor and the like, containing, as an active ingredient, at least one compound selected from the group consisting of a coumarin derivative represented by formula [where in the formula (I), R1 and R2, which may be identical with or different from each other, each represent a hydrogen atom or a group represented by formula (II) (where in the formula (II), R3 represents a linear or branched alkyl or alkenyl group having 1 to 20 carbon atoms)] and pharmacologically acceptable salts thereof.
CN102793696A Application of butylphthalide in preparation of medicament for treating bronchial asthma The invention provides novel medical application of butylphthalide, i.e. the application of the butylphthalide in the preparation of a medicament for treating the bronchial asthma. The experimental research on the spasmolysis of the butylphthalide on the isolated tracheal smooth muscle of a guinea pig and the influence of the butylphthalide on the incubation period of asthma of the guinea pig shows that the butylphthalide in the concentration range of 3.68*10-6 to 3.68*10-4g/mL has obvious spasmolysis on the tracheal smooth muscle of the guinea pig in the isolated spasticity caused by 5*10-6g/mL of acetylcholine or histamine. On the basis of continuously applying the butylphthalide to the guinea pig which is sensitive for the acetylcholine and the histamine for 10 days, a mixture of the acetylcholine and the histamine is atomized and sucked and the incubation period of asthma is observed. A result shows that 30 mg/kg and 90 mg/kg of butylphthalide has an effect of relieving the tracheospasm of the guinea pig, which is caused by the acetylcholine and the histamine. Therefore, the butylphthalide has a treatment effect on the asthma guinea pig and the treatment effect of the butylphthalide on the asthma guinea pig is related to the effect of inhibiting Ca2+ inner flow and expanded tracheal smooth muscle of the butylphthalide.
US7820722 Comprises a multi-carbon backbone having an at least partially neutralized carboxy or sulfonic functional group and also one or more side chains that have one or more carbon atoms and, optionally, one or more functional groups. A pharmaceutical composition comprising a drug and a permeation enhancer that comprises a multi-carbon backbone having a functional group and also one or more side chains which have one or more carbon atoms and, optionally, one or more functional groups.
US7279488 For therapy of acute inflammatory diseases: Septic shock, sepsis, SIRS, hemorrhagic shock, shock states induced by cytokine therapy (IL-2, TNF), organ transplantation and transplant rejection, head trauma, acute lung injury, ARDS, inflammatory skin conditions such as sunburn, inflammatory eye conditions The compounds of Formula (I) in which R1, R2, R3, R4, R5 and A have the meanings as given in the description are novel effective iNOS inhibitors.
CN102949342A Transdermal absorption pharmaceutical composition containing testosterone The invention provides a transdermal absorption pharmaceutical composition containing testosterone. The pharmaceutical composition is composed of male sex hormone used as an active component and one or a plurality of pharmaceutical adjuvants pharmaceutically applicable to a transdermal delivery system. The pharmaceutic adjuvants pharmaceutically applicable to the transdermal delivery system comprise a penetration enhancer and one or a plurality of alcohols which is in a liquid state under normal temperature. The male sex hormone is testosterone, dihydrotestosterone, methyltestosterone, testosterone propionate and testosterone undecanoate, and preferably, testosterone and dihydrotestosterone.
US20100062064 Method for Delivering A Pharmaceutical Composition to Patient in Need Thereof The present disclosure is directed to a method for delivering a pharmaceutical composition to a patient in need thereof, comprising: administering to said patient a pharmaceutical composition in unit dose form comprising naproxen, or pharmaceutically acceptable salt thereof, and esomeprazole, or pharmaceutically acceptable salt thereof
WO2005062897A3 Polymorphs of ezetimibe and processes for the preparation thereof The present invention relates to novel crystalline forms and amorphous form of Ezetimibe and the processes for the preparation thereof.
CN101724003A Ginsenoside Rg1 containing impure notoginsenoside R1 The invention discloses an effective component of standard ginsenoside Rg1, which is characterized by comprising ginsenoside Rg1 the content of which is greater than or equal to 90% and is smaller than 100% and impure notoginsenoside R1 the content of which is greater than or equal to 0.1% and is smaller than or equal to 9%; or, the content of the impure notoginsenoside R1 is greater than or equal to 1% and is smaller than or equal to 8%; or, the content of the impure notoginsenoside R1 is greater than or equal to 3% and is smaller than or equal to 6%; and pharmacological experiments show that the effective component of the standard of the application has a very good pharmacological action, and a main component has a synergistic action with an impurity and can be used as the raw material of the medicine of a medicine preparation.
US20090023737 Imidazo-Pyridazines, Triazolo-Pyridazines and Related Benzodiazepine Receptor Ligands Compounds of the Formula: are provided, as are methods for their preparation. The variables Z1, Z2, R3, Z4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
WO2013126707A1 Medical training kits and methods to simulate treatment of uncontrolled hemorrhage Medical training kits and methods include a simulated liquid blood which simulates mammalian whole blood and a simulated hemostatic component. The simulated liquid blood includes a gellable component, and a simulated hemostatic component includes a gelling agent. The gelling agent causes the gellable component in the simulated liquid blood to form a mass of semi-solid or solid material in response the simulated blood being brought into contact therewith to thereby simulate blood clotting. In certain embodiments, the gellable component is chitosan and/or an alginate compound and the gelling agent is at least one compound which causes the gellable component to desolubulize, polymerize, complex, precipitate, cross-link and the like so as to form a semi-solid or solid mass of chitosan in response to physical contact between the simulated blood and the simulated hemostatic agent.
CN1817861A Benzyloxy-substituted tryptophan derivative, its analogs, production and use thereof A benzyloxy-substituted tryptophan derivate, its analogs, production and use are disclosed. In chemical formula, Ar is phenyl, R1=benzoyl or chlorine-substituted benzoyl or phenylacetyl or propionyl and R2=hydrogen or carboxyl. It can be used for PPAR gamma agonist and medicine treating II-type diabetes. It has excellent conjugate activity.
WO2013063017A1 Diagnosis and treatment of mesothelioma This disclosure provides methods for surveillance, early detection and diagnosis, subtype classification, prediction of recurrence, prognosis and therapy of malignant mesothelioma based on profiles of indicator mutations in disclosed genes.
DE102006050026A1 Use of lactic acid compounds as tumor necrosis factor-alpha blocker, e.g. for suppressing immune system, for prophylaxis and/or treatment of autoimmune diseases and/or inflammatory diseases, preferably rheumatoid arthritis, spondylitis Use of lactic acid compounds (I) of formula (R2>-CH2-C(R3>)(R4>)-C (=O)-O-R1>) for the suppression of the immune system, is claimed. Use of compounds of formula (I) for the suppression of the immune system, is claimed. R1>alkyl-, alkenyl-, cycloalkyl-, alkoxyalkyl-, alkoxycarbonylalkyl- or aryl; R2>H, alkyl-, alkenyl-, cycloalkyl-, alkoxyalkyl-, alkoxycarbonylalkyl or aryl; either R3>-OH; and R4>H; or R3>-H and R4>-OH. - ACTIVITY : Immunosuppressive; Antiinflammatory; Antiarthritic; Antirheumatic; Osteopathic; Antibacterial; Antimalarial; Cerebroprotective; Respiratory-Gen; Vasotropic; Gastrointestinal-Gen; Antiulcer; Antipyretic; Anabolic. - MECHANISM OF ACTION : Tumor necrosis factor-alpha blocker; Major histocompatibility complex molecule blocker; Interferon-gamma blocker. Tests details are described but no results given.
US20100144779 Marine Alkalod Makaluvamines and Derivatives Thereof The present disclosure provides compounds based on the marine alkaloid makaluvamine. Described are compounds of the general formula (I) and (II). Also described are pharmaceutical compositions comprising one or more of the compounds of the general formula (I) and (II). The compounds and pharmaceutical compositions described inhibit the growth of several cancer lines, induce apoptosis and cell cycle arrest, display topoisomerase II inhibitory activity and modulate the activity and/or expression of key proteins involved in the regulation of cell growth. Methods of treatment and prevention using the compounds and pharmaceutical compositions described are also provided.
US20050131064 Administering powder or aerosol to nasal mucous membrane The present invention is directed to the treatment of cystic fibrosis that involves administration of a nitrosylating agent, such as S-nitrosoglutathione or ethyl nitrite.
US20120308669 Chocolate candies fortified with natural amino acids and/or herbal nutrients for relief of insomnia, pms, and difficulty concentrating A confection, such as chocolate, can be formulated to include naturally occurring amino acids and/or herbal extracts and/or plant extracts incorporated therein. The formulation allows a consumer to relieve health issues in a convenient, enjoyable manner. By incorporating the appropriate amino acids/herbal and plant extracts into a chocolate candy form, the confections can be formulated to provide relief of various ailments, such as insomnia, fatigue, PMS, difficulty concentrating and the like.
US20070287710 Piperidinediyl-containing sulfonamide; NPY Y5 receptor antagonist activity; antiobesity agent or anorectic agent The present invention provides a compound of the formula (I): (wherein, R1 is ethyl optionally substituted by halogen or amino optionally substituted by lower alkyl, R2 and R3 are each independently hydrogen or lower alkyl, X is cycloalkylene, lower alkylene or piperidinediyl, Z is optionally substituted phenyl or optionally substituted heterocyclyl) prodrug, pharmaceutically acceptable salt or solvate thereof.
EP1114166B1 Method for down-regulating osteoprotegerin ligand activity The invention provides a novel method for down-regulating the biological activity of osteoprotegerin ligand (OPGL, TRANCE) thereby rendering possible the treatment/amelioration of diseases characterized by excessive loss of bone mass, e.g. osteoporosis. Down-regulation is effected by inducing an immune response against OPGL in an individual in need thereof. Immune responses can be raised by classical immunization with immunogenic variants of OPGL or by nucleic acid immunization where the nucleic acids encode the OPGL variant. The invention also pertains to compositions, polypeptides and nucleic acids useful in the invention, as well as to vectors and transformed host cells useful in the preparation thereof.
US20090069282 Alkyne compounds with mch antagonistic activity and medicaments comprising these compounds The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
US7176204 Substituted carboxylic acid derivatives Novel substituted carboxylic acid derivatives which bind as ligands to human peroxisome proliferator activated receptor (PPAR) to activate the receptor and thereby exhibit potent effects of decreasing neutral fat, cholesterol, and blood sugar; and a processes for preparing the derivatives. Specifically, substituted carboxylic acid derivatives represented by general formula (1), and pharmaceutically acceptable salts and hydrates of the derivatives, and a processes for preparing the derivatives, the salts, or the hydrates
US20090318558 Solvent system of hardly soluble drug with improved dissolution rate The present invention relates to a solvent system with improved disintegration degree and dissolution ratio of a hardly soluble drug by highly concentrating the drug through partial ionization, and by establishing optimal conditions for enhancing bioavailability of the drug, such as the co-relation between the acid drug and the accompanied components, ionization degree of a solvent system, use of an appropriate cation acceptor, water content, selection of optimal mixing ratio of the respective components and use of specific surfactants, and to a pharmaceutical preparation comprising the same. The solvent system of the invention has advantages in that it can enhance bioavailability by improving the disintegration degree and dissolution ratio of a hardly soluble drug and also provide a capsule with a sufficiently small volume to permit easy swallowing.
CN103550158A Emodin solid dispersion, drug-containing pellet core, colonic targeted micropill, and applications of three The invention relates to emodin solid dispersion, a drug-containing pellet core, a colonic targeted micropill, and applications of the three. The emodin solid dispersion is prepared from emodin and a carrier material, wherein the carrier material is one or several selected from poloxamer 188, poloxamer 407, Kollidon 12 PF, Kollidon VA 64, Kollicoat IR or Soluplus, and the weight ratio of emodin to the carrier material is 1:2-1:15. The drug-containing pellet core and the colonic targeted micropill both contain the emodin solid dispersion. The emodin solid dispersion is substantially improved in solubility of indissolvable drug emodin; and the targeted micropill helps to realize colonic positioning release in vivo/vitro of emodin, and has substantial protective effect on intestinal barrier of a rat severe acute pancreatitis pancreatitis model.
CN101890021A Cefozopran hydrochloride for injection and preparation method thereof The invention belongs to the field of medical preparations, and relates to cefozopran hydrochloride for injection and a preparation method thereof. The cefozopran hydrochloride for injection comprises the following components in part by weight: 200 to 1,000 parts of cefozopran hydrochloride, 350 to 2,000 parts of soybean lecithin, 150 to 450 parts of cholesterol, 45 to 100 parts of anhydrous sodium carbonate and 25 to 85 parts of glucose. The cefozopran hydrochloride for injection can achieve better treatment effect on the basis of low content of a main ingredient, and simultaneously reduces the incidence rate of untoward effect, so the product is more safe and effective.
DE102008050591A1 Beverage, useful to promote dental health of children, comprises sugar-free teas, e.g. rooibos tea, and sugar substitute, e.g. xylitol, which inhibits growth of cariogenic microorganisms Beverage comprises sugar-free teas, preferably rooibos tea, and at least one sugar substitute, preferably xylitol, which inhibits growth of cariogenic microorganisms.
WO2011059969A3 Mammalian metabolites of steroids Described herein, in certain embodiments, are steroidal derivatives, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions.
US6855723 Methods of modulating serine/threonine protein kinase function with azabenzimidazole-based compounds The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with azabenzimidazole-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to azabenzimidazole compounds and pharmaceutical compositions comprising these compounds.
US20080188488 Heterocyclic Derivatives and Their Use as Stearoyl-Coa Desaturase Inhibitors Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, J, K, W, V, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
WO2011105825A3 Resveratrol effective in treating and preventing prion diseases The present invention relates to resveratrol effective in treating and preventing prion diseases, and more particularly, to a composition containing resveratrol as an active ingredient for the treatment and prevention of prion diseases. According to the present invention, the resveratrol of the present invention has the effect of protecting nerve cells. When the resveratrol of the present invention was used to treat nerve cells, it increased the expression and activity of sirtuin 1 in nerve cells, and protected nerve cells from the cytotoxicity of prions, thereby inhibiting cell apoptosis. Accordingly, a composition containing resveratrol of the present invention as an active ingredient, as a composition for the prevention and treatment of prion diseases, can be used as a medication that is easy to administer to humans, and can be developed into a feed additive to be easily administered to livestock.
US20110165247 Device for the transdermal administration of a rotigotine base The invention relates to a polymer matrix suitable for the transdermal administration of rotigotine [(−)-5, 6, 7, 8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphtol], containing a matrix for the transdermal administration of rotigotine [(−)-5, 6, 7, 8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1 naphtol], containing a matrix polymer which is supersaturated with a rotigotine base. Said polymer matrix is characterised in that the part of the rotigotine which is not dissolved in the matrix polymer is dispersed in the matrix polymer as amorphous particles having a maximum mean diameter of 30 ?m, and the matrix is free of solubilisers, crystallisation inhibitors and dispersants. The invention also relates to a flat device for the transdermal administration of rotigotine, containing the above-mentioned, preferably silicon-based polymer matrix which is supersaturated with rotigotine, and a rear layer which is impermeable to the active ingredient.
CN102690309A Floxuridine compound and preparation method and application thereof The invention relates to the medicine technology field, and relates to a floxuridine compound with antitumor activity, a preparation method, and an application in preparation of antitumor drugs thereof. Experiments show that the compound of the invention, compound crystals or its medicinal salts can prevent intestinal toxicity of 5'-deoxy-5-floxuridine, and an enzyme (dThdPase) related to the compound has a higher concentration in tumor tissue than in normal tissue. Therefore, the compound of the invention or its medicinal salts can be used for preparing antitumor drugs.
WO2009020028A1 Determination and suppression of expression level of g protein-coupled receptor kinase 4 gene in breast cancer cell It was first discovered that GRK4 is highly expressed in a human breast cancer cell, and it is intended to provide a primer set having specific sequences capable of determining the expression level of a GRK4 gene by PCR, and GRK4 siRNA capable of suppressing human breast cancer cell proliferation. As means for resolution, the sequences of the primer set specific for the GRK4 gene for PCR are represented by SEQ ID NOS: 1 and 2, and the sequences of a double-stranded RNA for siRNA are represented by SEQ ID NOS: 3 to 8.
WO2011040212A1 Therapeutic agent for brain tumor The present invention relates to an agent for the prophylaxis or treatment of metastatic tumor that has spread to the brain from other tissue, comprising N-{2-[4-({3-chloro-4-[3-(trifluoromethyl)phenoxy]phenyl}amino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl]ethyl}-3-hydroxy-3-methylbutanamide or a salt thereof.
WO2012051941A1 Uses of 15-benzylidene-14-deoxy-11,12-dehydroandrographolide derivatives in the preparation of antineoplastic drugs Disclosed in the present invention are applications for 15-benzylidene-14-deoxy-11, 12-dehydroandrographolide derivatives in the preparation of antineoplastic drugs.
CN1615893A Prescription of compound skeletal musle relaxant and analgesic containing etezamide and its preparing method The present invention relates to compound skeletal muscle relaxant analgetic. The compound skeletal muscle relaxant analgetic contains etenzamide and one or several of the medicines selected from chlorzoxazone, methocarbamol and caffeine, as well as disintegrating agent, adhesive, lubricant and surfactant. It is prepared into tablet.
CA2822490A1 Nutritional compositions comprising human milk oligosaccharides and nucleotides and uses thereof for treating and/or preventing enteric viral infection Disclosed are nutritional compositions including human milk oligosaccharides and nucleotides that can be administered to preterm infants, term infants, toddlers, and children for reducing inflammation and the incidence of inflammatory diseases.
WO2007147133A1 Stabilized tetracycline compositions The invention provides a package that comprises a first rapidly disintegrating dosage form comprising tetracycline, and a second rapidly disintegrating dosage form that comprises a buffer. The invention also provides methods for treating or preventing mucositis, comprising mixing the dosage forms of the package in an aqueous medium to form a solution or suspension, and administering the solution or suspension topically to the oral cavity of a patient. The invention further provides an aqueous formulation comprising the first and second dosage forms in an aqueous medium.
WO2006061233A1 The use of medicament 4-(s)-(4-acetyl-piperazin-1-yl)-2-(r)-(4-fluoro-2-methyl-phenyl)-piperidine-1-carboxylic acid, [1-(r)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide The present invention relates to a new medical use 4-(S)-(4-Acetyl-piperazin-1-yl)-2-(R)-(4-fluoro-2-methyl-phenyl)-piperidine-1-carboxylic acid, [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide or pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing it, in the treatment of overactive bladder.
EP2533775A1 Carbonic anhydrase inhibitors A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R-NH-CX-NH-(CH2)n-Ar-Q-SO2-NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n = 0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.
CN1844139A Triterpene compounds with ring breakage in C3 and C4 position and their use for prevention and treatment of AIDS The invention relates to a C3,4 position broken-ring triterpenoid extracted from medicinal herb plant of Kadsura, experimental investigation shows that, the compounds have evident inhibitory action to AIDS virus, and the toxic and side effects are low.
CN101822666A Application of benzoyl silibinin for preparing medicaments for treating viral hepatitis B The invention relates to application of benzoyl silibinin for preparing medicaments for treating viral hepatitis B, in particular to application of 23-bit 3,4-dimethoxy-benzoyl substituted silibinin ester or medicinal salts thereof for preparing medicaments which are used for eliminating Hepatitis B virus surface antigen (HBsAg) and hepatitis B e antigen (HBeAg) and inhibiting HBV (Hepatitis B Virus) DNA replication. The compound plays an extremely remarkable role in inhibiting HBsAg and HBeAg activities, and the strengths for eliminating the HBsAg and the HBeAg under the concentration of 20 micrograms/ml in the compound are respectively 93.3 percent and 91.2 percent; meanwhile, the compound displays more than 99 percent of inhibition ratio to HBV DNA under the concentration of 20 micrograms/ml and has 23 percent of inhibition ratio higher than that of positive control medicine Lamivudine and 2.6 times higher than that of Alpha-interferon. Results indicate the application of flavone lignans and medicinal salts which are expectedly used for preparing non-nucleoside medicaments for eliminating the HBsAg and the HBeAg, inhibiting HBV DNA replication and treating hepatitis B virus infection diseases.
US20130039987 Method for increasing the solubility of a transcriptase inhibitor composition The invention provides a method for increasing the solubility of nevirapine, including the steps of rendering nevirapine in a gaseous phase; and rendering the gaseous phase in a relatively more soluble solid particulate form. The invention further provides for a crystalline Form-VI (36) of nevirapine having an X-ray diffraction pattern of (2-theta values in degrees) 9.2953, 11.2023, 12.7019, 12.9796, 13.5273, 15.4670, 17.2597, 19.1038, 19.7267, 21.1303, 22.9381, 25.5589, 26.4913, 27.2150, 27.7283, 29.7134, and 33.8343 degrees two theta. The invention further provides for the preparation of microspherical and/or nanospherical Form-V (34) and crystalline Form-VI (36) of nevirapine as well as novel dosage forms including parenteral-, inhalant-, transdermal- and oral dosage forms.
CN101475599B Novel method for synthesizing antineoplastic medicament nedaplatin The invention relates to a method for preparing an antitumor drug of carboplatin H12C6O4N2Pt. The method comprises the following steps: using cis-diiododiammineplatinum (II) as a reactant, adding water and uniformly stirring, heating to 50-60 DEG C by a water bath, avoiding light, slowly adding Hg2CBDCA, reacting for 8-10h and filtering, concentrating the filtrate under reduced pressure and obtaining the carboplatin solid. The molar ratio of Pt(NH3)2I2 to Hg2CBDCA is equal to 1:1. The method for preparing the carboplatin has short prcess, avoids the impurity of Ag<+> introduction. At the same time the solubility product of the HgI is small, so that the HgI is easy to remove, the yield of the target product is high up to more than 80%, wherein the CBDCA is used to substitute the 1,1-cyclobutanedicarboxylic radical.
US6905701 Formulations for transmucosal vaginal delivery of bisphosphonates Devices, methods, and improved formulation for transmucosal vaginal delivery of bisphosphonates. A targeted site delivery of bisphosphonates to the systemic circulation using a vaginal device comprising an improved bisphosphonate formulation for transmucosal delivery. A method for treatment of osteoporosis and related bone and skeleton diseases, for prevention of bone breakdown and loss of bone mass and strength by intravaginal administration of bisphosphonates to the vagina and transmucosal delivery of bisphosphonates to the general circulation.
WO2012154627A2 Light delivery device and related compositions, methods and systems Devices and systems for delivering light to a target are described. Methods of using such light delivery device and system are also described. A method of using a photosensitizing compound with the light delivery device is also described.
CN103349666A Pharmaceutical composition injection of compound liposoluble vitamin and preparation method thereof The invention provides a pharmaceutical composition injection of a compound liposoluble vitamin. The injection comprises the following raw materials: 0.5-1 g vitamin A palmitate, 0.001-0.005 g vitamin D2, 5-10g Vitamin E, 11.0+/-0.1 g vitamin K, 50-80 g Solutol hs15, and a proper amount of liposoluble antioxygen, and 1 000 ml injection can be obtained. The pharmaceutical composition injection of the compound liposoluble vitamin can be placed in the ordinary-temperature and ordinary-state environment, is always in the clear state within the normal guarantee period, and is free from unstable phenomena of particles, muddiness, layering and the like.
CN103230396A New application of Rapamycin The invention relates to an application of Rapamycin in preparation of medicines for relieving inflammatory pain. Thirty minutes before BmKI injection, three dosages of Rapamycin are injected to a gap between intrathecal L5-L6 sacrums of a rat, so as to research the relieving effects of different dosages of Rapamycin on experimental spontaneous pain, paroxysmal grand mal in sense of pain, double-side mechanical pain, single-side heat pain and the like. The new application of Rapamycin provided by the invention is built on the basis of an experimental animal inflammatory pain model and provides grounds for researching an analgesic molecular mechanism associated with an mTOR signal path and developing novel analgesic pains.
CN101518531B Analgesic anti-inflammatory composite medicament and method for preparing same The invention discloses an analgesic anti-inflammatory composite medicament made from lappaconitine and tetrahydropalmatine, a patch made from the composite medicament and a method for preparing the pThe invention discloses an analgesic anti-inflammatory composite medicament made from lappaconitine and tetrahydropalmatine, a patch made from the composite medicament and a method for preparing the pastrointestinal tracts are avoided, the toxicity and the side effect of the composite medicament are reduced, and the bioavailability and the safe curative effect of the composite medicament are imo gastrointestinal tracts are avoided, the toxicity and the side effect of the composite medicament are reduced, and the bioavailability and the safe curative effect of the composite medicament are improved. The composite medicament is convenient to use without causing patients to be afflicted by pain and is very effective in relieving pain and diminishing inflammation.proved. The composite medicament is convenient to use without causing patients to be afflicted by pain and is very effective in relieving pain and diminishing inflammation.atch. The patch comprises a back lining layer, a medicament storage layer and a protection layer, wherein the medicament storage layer is made from raw materials including the lappaconitine, the tetraatch. The patch comprises a back lining layer, a medicament storage layer and a protection layer, wherein the medicament storage layer is made from raw materials including the lappaconitine, the tetrahydropalmatine and pressure-sensitive adhesive; and the patch is made by adding a proper amount of transdermal enhancerfrom in to the same three raw materials. Experiments and clinical research provehydropalmatine and pressure-sensitive adhesive; and the patch is made by adding a proper amount of transdermal enhancerfrom in to the same three raw materials. Experiments and clinical research provethat the composite medicament made from raw medicament materials of lappaconitine and tetrahydropalmatine according to a certain proportion can reduce the toxicity of the lappaconitine and improve thethat the composite medicament made from raw medicament materials of lappaconitine and tetrahydropalmatine according to a certain proportion can reduce the toxicity of the lappaconitine and improve the median lethal dose (LD 50). Due to the use of the patch made from the composite medicament, the blood concentration can be kept stable for a long time, the first-pass effect on liver and the damage tmedian lethal dose (LD 50). Due to the use of the patch made from the composite medicament, the blood concentration can be kept stable for a long time, the first-pass effect on liver and the damage to g
WO2014096454A1 Soluble, dispersible or orodispersible tablets comprising cyclophosphamide The present invention concerns a soluble tablet, which comprises : (a) cyclophosphamide, a hydrate form thereof, a pharmaceutically acceptable salt thereof, or any mixture thereof, in an amount ranging from 1 to 1 5 % by weight on a cyclophosphamide active weight basis, and (b) from 10% to 99 % by weight of a solubilising agent chosen from disaccharides, sugar alcohols that are solid at ambient temperature, and mixtures thereof. The tablets of the invention can be dispersed in water, and allow to administer cyclophosphamide in a safe and reliable manner. They are particularly suitable for treating paedriatric cancer. They can also be dissolved in saliva.
EP2438921A1 23-O-Acetylshengmanol-3-O-beta-D-xylopyranoside and its medical use The present invention relates to 23-O-acetylshengmanol-3-O-β-D-xylopyranoside or a compound of formula (I) for use as a medicament, and pharmaceutical compositions comprising that compound, in particular for use as an anxiolytic agent, a sedative agent, a hypnotic agent, an anticonvulsant agent, an analgesic agent, an anesthetic agent, an antiepileptic agent, and/or a muscle relaxant.
US20050148582 N-[1-butyl-4-piperidinylmethyl[3,4-dihydro-2 oxazino[3,2-a indole-10 carboxamide as drugs with Cahpo4 or Ca3/po4/2 fillers or binders for use in treatment of irritable bowel syndrome, urinry incontience or arrhythmias A pharmaceutical composition comprising N-[(1-nbutyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide (SB 207266) or a pharmaceutically acceptable salt thereof in combination with one or more pharmaceutically acceptable carriers, wherein at least some of the SB 207266 or salt thereof is in granulated form. Preferably, a filler and/or binder are also present.
CN101352448A Use of Liriope muscari Bailey C in pharmacy The invention belongs to the field of pharmacy, and discloses the application of rusogenin fucopyranoside C in the pharmacy. The invention also provides the application of the rusogenin fucopyranoside C in the preparation of the medicine for resisting tumor metastasis, and more particularly relates to the application in the preparation of the medicine for generating tumour new blood vessels and inhibition of relative tumor metastasis. Being proved by the study of the invention, the rusogenin fucopyranoside C can effectively inhibit the growth, migration and adhesive ability, can inhibit lung metastasis of melanoma B16, and provides new selection in the application of preparing the medicine for resisting tumor metastasis.
US20080008771 Nitric Oxide Dioxygenase Inhibitors A method and composition to inhibit the enzyme nitric oxide dioxygenase (NOD) and therefore accumulate nitric oxide (NO) in cells or tissues. By preventing NO removal, the inhibitors may effect cellular signaling, modulate vasotension, enhance O2 delivery to tissues, and provide antibiotic and/or antineoplastic effects. Inhibitors include compounds that bind to the iron in the heme portion of NOD, and include allicin and azoles.
US20090197926 Benzimidazoles and their use for the treatment of diabetes Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein: R1 is selected from optionally substituted phenyl, cyclopentyl, cyclohexyl and 5- or 6-membered heteroaryl; L1 is a direct bond or a linker selected from, for example, —O—, —OCH2— and —CH2O—; R2 is selected from, for example, (3-6C)cycloalkyl, (5-12C)bicycloalkyl, phenyl and a 4, 5- or 6-membered saturated, partially or fully unsaturated heterocyclyl ring; wherein R2 is substituted by defined substituents and R6 is selected from, for example, hydrogen, fluoro and chloro; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
US20070212714 Novel genes TZap7/A, TZap7/B and TZap7 involved in T cell activation and uses thereof Described are generally immune response cDNA TZap7/A, TZap7/B and TZap7 polynucleotides encoding novel proteins involved in modulation of immune responses and antibodies recognizing said proteins. Furthermore, vectors comprising the aforementioned polynucleotides and host cells transformed therewith as well as their use in the production of the above-defined proteins are described. Additionally, pharmaceutical and diagnostic compositions are provided comprising any one of the afore-described polynucleotides, vectors, proteins, or antibodies. Furthermore, methods and uses for modulating immune responses through the novel TZap protein as well as pharmaceutical compositions comprising agents which act on the TZap protein or its ligand are described. Also, the use of said polynucleotides, vectors, proteins or antibodies for the preparation of diagnostic and pharmaceutical compositions for use in organ transplantation, for the treatment of autoimmune, allergic or infectious diseases, or for treatment of tumors is provided.
US20090227644 Agent for regeneration and/or protection of nerves An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system.
CN101797389A Method for preparing colon cancer chemotherapy medicament The invention provides a method for preparing colon cancer chemotherapy medicament, which comprises the following steps: weighting the raw material of plasma in the blood bank, centrifuging the plasma, adjusting the density of the plasma, and extracting low-density lipoprotein from the plasma; purifying the low-density lipoprotein to obtain the carrier of the target medicament; compounding the low-density lipoprotein with the target aclacinomycin medicament for treating colon cancer; and injecting the compound of the low-density lipoprotein and the target aclacinomycin medicament into the body of the patient whose blood type is the same as the raw material of plasma to treat the colon cancer. The clinical practice shows that the injection of the compound of the low-density lipoprotein and the target aclacinomycin medicament has the satisfactory effect for treating the colon cancer clinically and can not cause obvious toxic and side reaction of chemotherapy. Used for treating the colon cancer of 185 patients, the injection of the compound of the low-density lipoprotein and the target aclacinomycin medicament achieves the effective rate of 100 percent and the survival rate of more than 96 percent in three years, thereby having high popularization and application values.
CA2854424A1 Substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with an so2-containing group as vanilloid receptor ligands The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with a S02-containing group as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
WO2005114206A3 Diagnostics and therapeutics for diseases associated with serotonin 5-ht5a receptor (5ht5a) The invention provides a human 5HT5a which is associated with the cardiovascular diseases, infections, gastroenterological diseases, cancer, inflammation, metabolic diseases, hematological diseases, neurological diseases, urological diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular diseases, infections, gastroenterological diseases, cancer, inflammation, metabolic diseases, hematological diseases, neurological diseases, urological diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of 5HT5a as well as pharmaceutical compositions comprising such compounds.
WO2006037032A3 Prodrugs of protein tyrosine kinase inhibitors Novel compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as oncologic and immunologic disorders.
WO2005002624A1 Prolyl oligopeptidase inhibitors ameliorating recovery from brain trauma The present invention relates to a method for the treatment of sensorimotor dysfunctions caused by brain trauma with an inhibitor of prolyl oligopeptidase or a pharmaceutically acceptable ester or salt thereof.
CN102210765B Orally-taken Chinese medical decoction for treating lung meridian wind-heat type nasosinusitis The invention discloses an orally-taken Chinese medical decoction for treating lung meridian wind-heat type nasosinusitis, which is characterized by being prepared from the following Chinese medical raw materials in percentage by weight: 5.9-7.2% of ephedra, 5.9-7.2% of almond, 17.6-21.6% of raw gypsum, 5.9-7.2% of licorice, 8.8-10.8% of herba schizonepetae, 3-3.6% of radix sileris, 8.8-10.8% of magnolia flower, 5.9-7.2% of radix angelicae, 3-3.6% of peppermint leaf, 5.9-7.2% of notopterygium root, 3-3.6% of asarum, 5.9-7.2% of xanthium, 5.9-7.2% of chuanxiong rhizome and 4.9-6.0% of cicada slough. The Chinese medical decoction has the functions of freeing the lung, clearing away heat, dredging the nasal cavity, dispelling wind, expelling cold, dissipating blood stasis, eliminating pus, resisting allergic reaction, relieving toxicity, diminishing inflammation and promoting tissue regeneration; and the Chinese medical decoction has the advantages of strong pertinence, high effect taking speed, short treatment time, good treatment effect, simple formulation, easy material acquisition and low treatment cost, wherein the cure rate is 84.6%, and the effective rate is 100%.
CN103054192A Healthcare cigarette holder The invention provides a healthcare cigarette holder comprising a cigarette holder body, a smoking quitting inner core storage tube and a cigarette connecting tube. By the aid of a series of cigarette holders for step-by-step smoking quitting, smoking quitting requirements of smoking quitters can be met, and the smoking quitters can go through physiological and psychological dependence periods smoothly and painlessly.
DE102006016365A1 Composition for inhibiting expression of one or more target genes in a eukaryotic cell comprises one or more genetic constructs comprising a target gene and a small interfering RNA tag Composition for inhibiting expression of one or more target genes in a eukaryotic cell comprises one or more genetic constructs comprising a target gene and a small interfering RNA (siRNA) tag, each tag having a different nucleotide sequence. An independent claim is also included for inhibiting expression of a target gene in eukaryotic cells by transfecting the cells with a composition as above and introducing a small interfering RNA complementary to the tag.
WO2014023813A1 Alkylpyrimidine derivatives for the treatment of viral infections and further diseases This invention relates to alkylpyrimidine derivatives of formula (I), processes for their preparation, phamaceutical compositions, and their use in therapy for the treatment of viral infections.
WO2005105120A2 Pharmaceutical combination, active on central nervous system (cns) and set of pharmaceuticals; method of treatment of cns-disorders; means facilitating penetration of the hematoencephalic barrier; pharmaceutical means for endonasal administration The invention relates to the field of pharmacology and refers to pharmaceuticals, having effect upon the central nervous system, - specifically, to pharmaceutical combination usable to treat CNS functional disorders. The objective is creation of an efficacious pharmaceutical combination, containing the main pharmacologically active substances in concentration and dosage lower than those usually administered, and producing as few side effects as possible; development of a method for correction of conditions connected with CNS functional disorders and involving the proposed pharmaceutical combination; creation of a set of pharmaceuticals containing the developed pharmacological combination; identification of new application for active forms of oxygen and creation of a pharmaceutical means facilitating penetration of the hematoencephalic barrier by medicinal substances and/or metabolites. For this purpose, claimed is a pharmaceutical combination, which has effect over CNS functioning, which comprises at least one compound having therapeutic effect on the CNS, and a compound, facilitating penetration of the hematoencephalic barrier by the former; as the compound facilitating penetration of the hematoencephalic barrier the pharmaceutical combination comprises means for endonasal administration, which has reflectory (mainly neuro and vasoactive) effects over structures and receptors of nasal mucous membrane, mainly receptors of vomeronasal systems and trifacial nerve.
WO2010132554A3 Diaza heterocyclic compounds for phototherapy The invention relates generally to optical agents, including phototherapeutic agents, for biomedical applications, including phototherapy. The invention includes optical agents, and related therapeutic methods, comprising alicyclic diaza compounds, incuding 1,2 diaza heterocyclic compounds, having a photolabile N-N bond directly or indirectly linked to at least one carbocyclic aromatic and/or heterocyclic aromatic group. In some embodiments, for example, the invention provides alicyclic diaza compounds for phototherapeutic methods having a photolabile N-N bond that undergoes photoactivated cleavage to produce reactive species, such as radicals, ions, etc., that achieve a desired therapeutic effect, such as selective and/or localized tissue damage and/or cell death.
US7888510 1,4-disubstituted piperidine compounds like N-(9-Ethyl-9H-carbazol-3-yl)-2-[4-(2-hydroxymethyl-6-methyl-phenylamino)-piperidine-yl]acetamide; chloroacetyl chloride is reacted with respective compounds in the presence of dichloromethane and triethylamine or diisopropylethylamine It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man. Said object was achieved by providing 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1.
CN1895422A Chinese animal medicinal composition for treating fowl colibacillus and its making method A Chinese veterinary medicine for treating the colibacillosis of fowls is prepared from 4-14 Chinese-medicinal materials including rhubarb, scutellaria root, coptis root, phellodendron bark, etc.
US20110172242 Treatment of organophosphate exposure with tetrahydroindolone arylpiperazine compounds A method of treating exposure to organophosphate agents through the use of compounds comprising tetrahydroindolone and arylpiperazine moieties.
CN101732594A Powder for burns and scalds The invention relates to powder for burns and scalds. The medicament is prepared by preparing, fire attack and refining a composition taking 10 grams of toilet paper, 89.5 grams of cane sugar and 0.5 gram of bulbus fritilariae as raw materials, and the percentages of the raw materials are: 10 percent of bamboo-made toilet paper, 89.5 percent of f cane sugar and 0.5 percent of bulbus fritilariae. Fritillaria is crushed to be fine powder mixed well with sugar; the toilet paper is put on a plank flat; 25 grams of mixed sugar raw material is scattered on the edge of the toilet paper in a straight line in order to rub and roll the toilet paper to be a strip; 20 strips are put in an iron pot as a bundle and burnt; the obtained product is crushed to be grains like flour in a pulverizer and the iron pot after fire naturally goes out; and pure rapeseed oil and medicinal powder are mixed in a ratio of 7:3, namely 70 percent of medicinal powder and 30 percent of oil. In order to save cost, oil medicinal powder is diluted and stirred to be paste smeared on a wound according to the size of the wound once to twice a day to keep the wound with the medicament, and after diluted medicinal solvent is smeared, the wound needs no dressing change or dressing. The medicament has the effects of relieving pain, moistening skin, promoting tissue regeneration, preventing suppuration, eliminating swellings and producing no toxic-side effects. The wound of which 80 percent of the surface is 1 to 5 millimeters in depth can be treated to heal within 15 days. A slight wound of which 40 percent of the surface is 1 to 3 millimeters in depth can be treated to heal within 8 days. Original skin color can be restored within 1 to 3 months without leaving any scars or color. The medicament has the advantages of excellent effect, low cost and capability of saving 50 percent of medical expense for patients.
EP1360508B1 Prediction of wound healing by urinary nitrate assay Wound healing is impaired in many diabetics, who suffer increased risk of chronic foot ulceration and imputation. Diabetic patients with poor healing ability were found to possess significantly lower fasting urinary nitrate levels than diabetic patients with normal healing ability or non-diabetic controls, implicating decreased endogenous nitric oxide activity as the mediator of diabetes-impaired wound healing. Methods and kits are provided for predicting the wound healing ability of diabetic patients and patients with venous stasis ulceration or another disease or condition characterized by chronically impaired cutaneous wound healing in some patients based on the levels of nitric oxide related products such as nitrate or nitrite in urine or other specimens. Methods are also provided for treating non-wound healing patients and monitoring diabetic ulcer treatment.
US20110014292 method of prophylaxis and agents for use therein The present invention relates generally to a method of prophylactically or therapeutically treating antigen-induced airway tissue inflammation and agents for use therein. More particularly, the present invention provides a method of prophylactically or therapeutically treating allergic airway inflammation and agents for use therein via the administration of the method of the present invention is useful, inter alia, in the treatment and/or prophylaxis of conditions characterised by antigen-induced airway tissue inflammation.
CN102775411A Aryl ethynyl benzamide compound used as protein kinase inhibitor The invention discloses a compound which is shown in a formula (I) and is used for treating or preventing diseases related to protein kinase, and a pharmaceutically acceptable salt or configurational isomer thereof. In the formula (I), the linking group L1, the ring A and the substituting groups Ra, Rb, Rc and Rd are as defined in the specification. The invention also discloses a preparation method of the compound shown in the formula (I), a medical composition containing the compound shown in the formula (I), and application of the compounds in the preparation of medicaments for preventing diseases related to protein kinase.
US20090221642 Muscarinic receptor agonists, compositions, methods of treatment thereof, and processes for preparation thereof-176 Compounds of Formula 1, or pharmaceutically acceptable salts thereof: wherein X, R1, R2, R3, R4, R5, n, m, and p are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
US8604055 Substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
US20110045052 Bioactive Glass Coatings The present invention relates to bioactive glass coatings. In particular, the present invention relates to bioactive glass coatings for Ti6Al4V alloys and chrome cobalt alloys, wherein the thermal expansion coefficient of the glass coating is matched to that of the alloy. Such coatings have a particular application in the field of medical prosthetics. The bioactive glass comprises (in mol %) 35-53 SiO2; 2-11 Na20; at least 2% of each of CaO, MgO and K20; 0-15 ZnO; 0-2 B202 and 0-9 P205.
WO2013059736A1 Methods and compositions for treating oral mucositis The present disclosure relates generally to the field of oral mucositis. More particularly, methods and compositions for treating, ameliorating and/or preventing oral mucositis are provided. Methods and compositions for treating, ameliorating and/or preventing oral mucositis are also provided.
CN102000049A Injection preparation containing etidocaine isomer The invention relates to an injection preparation containing an etidocaine isomer, which is prepared by taking an etidocaine optical isomer as well as adrenaline and pharmaceutical salt thereof as active components, and combining with a pharmaceutically suitable auxiliary material. The injection preparation can exist in forms of a water needle, freeze-dried powder, sterile powder and high-capacity infusion, and is used for infiltration anesthesia, nerve block, epidural anesthesia and superficial anesthesia.
US7081470 Use of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.
EP1567145B1 Analgesic uses of (s)-norketamine The present invention relates to norketamine and ketamine/norketamine prodrugs, and methods of their use and analgesics. More particulary, the invention relates to norketamine and N-conjugated prodrugs of ketamine and norketamine, and methods of using these agents for the management of chronic pain without requiring administration of narcotics. The invemtion relates to self-management of pain on an outpatient basis comprising administering via conventional routes, including transdermal, nasal, rectal, oral, transmucosal, intravenous, intramuscular, and other routes, one or more doses of norketamine and/or ketamine/norketamine prodrugs effective to alleviate pain to a subject suffering from pain.
WO2006083760A1 AMINO-PYRIDINES AS INHIBITORS OF β-SECRETASE The present invention provides an amino-pyridine compound of formula (I). The present invention also provides methods for the use thereof to inhibit β -secretase (BACE) and treat β -amyloid deposits and neurofibrillary tangles.
WO2014095798A1 Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists) A compound according to Formula (Ia), wherein Cy, L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula (I) that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis), lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
WO2012156917A2 Method for obtaining epsilon-viniferin and/or resveratrol and corresponding products The invention relates to a method for obtaining purified ε-viniferin (Vf-Dry) and/or resveratrol which has a low content or is even free of ε-viniferin (Rv-Dry), from an extract, which is crude (EBPS), dry (EBPS-dry), or in solution (EBPS-Sol), of a plant material rich in stilbenoid polyphenols, characterized in that it comprises at least one cycle of adsorption-desorption on a solid substrate such as poly(vinylidene fluoride) or PVDF with EBPS-Sol, and/or partition of this EBPS-Sol solution with ethyl acetate. Applications in particular in the cosmetics industry and in therapy.
US7071193 7-amino-2-alkylthiopteridin-4-yl-amines for the treatment of chemokine-related diseases Pteridine compounds of formula (I) processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in the treatment of inflammatory diseases such as psoriasis, rheumatoid arthritis, diseases in which angiogenesis is assocated with raised CXCR2 chemokine levels (diabetic retinopathy) and COPD. The compounds are ligands for chemokine receptors and medical indications mentioned in the description include: diseases of the respiratory tract (COPDD, asthma, bronchitis, rhinitis, fibroid lung, pneumonia, etc.), diseases of the bones and joints (arthritis, etc.), skin-diseases (psoriasis, etc), diseases of the gastrointestinal tract, diseases in other tissues and systemic disease (multipe sclerosis, atherosclerosis, AIDS, type 1 diabetes, leprosy, sepsis, etc.), allograft rejection, cancers, cystic fibrosis, stroke, burn wounds, skin ulcers, reproductive disease and more.
US20080292714 Bone targeting of degradable drug filled nanoparticles This invention provides a method of modifying a cellular response in a mammal. The method comprises administering to the mammal an effective amount of biodegradable nanoparticles, each of said nanoparticles comprising an active agent, a biodegradable polymer, and a bone targeting agent administering to a mammal an effective amount of a composition comprising a compound absorbed in a biodegradable nanoparticle which is attached to a bone targeting agent. The invention also provides a method for modifying a cellular response in a mammalian cell comprising contacting the mammalian cell with biodegradable nanoparticles. The invention further provides a method of delivering an exogenous substance to a mammal. The method comprises administering to the mammal a composition comprising the exogenous substance absorbed into a biodegradable nanoparticle, wherein the biodegradable nanoparticle is covalently attached to a bone targeting agent. The invention also provides a composition and a process for preparing the composition comprising a biologically active or therapeutic agent of compound, a biodegradable nanoparticle, and a bone targeting agent.
WO2006017406A1 Cyanoamidine p2x7 antagonists for the treatment of pain cyanoamidines compounds of formula (I) and (II) and their derivatives wherein R1 - R12 are as defined in the specification act as antagonists of the P2X7 receptor. These compounds are particularly useful in the treatment of pain, inflammation and neurodegeneration states.
CN102617576A 7-substituted-phenoxyl-[1,2,4]triazole[4,3-f]pyrimidine derivative used as anti-epileptic drug and medically-usable salt thereof A 7-substituted-phenoxyl-[1,2,4]triazole[4,3-f]pyrimidine derivative used as an anti-epileptic drug and a medically-usable salt thereof. The invention provides the 7-substituted-phenoxyl-[1,2,4]triazole[4,3-f]pyrimidine derivative which has small toxic and side effects, shows the value of usage as an anticonvulsant and has novel pharmacological properties and also provides an addition salt of medically-usable acid of the derivative. A compound as represented by formula I and an addition salt of medically-usable acid thereof are described in the specification, wherein R in the formula is selected from a variety of chloroalkanes. The compound has strong anticonvulsant activity, low toxic and side effects and a high safety index and lays a foundation for research and application of anti-epileptic drugs.
WO2013114390A1 Gastro retentive drug delivery system of calcium supplements Provided are a gastro retentive dosage form of calcium and salts thereof and preparing method thereof. Said dosage form comprises absorption enhancing agents, diluents, binders, disintegrants, floating agents, polymers, lubricants, anti adherents, preservatives and combinations thereof.
US8563556 Crystalline forms and two solvated forms of 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one lactic acid salts Crystalline forms or polymorphs of 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one lactic acid salts, as well as to methods of making the same, pharmaceutical compositions comprising the same and methods of treatment using the same.
WO2007016208A2 1,2-benzisoxazole-3-methane-sulfonic acid ammonium salt The present invention provides substantially isolated ammonium salt of 1,2- benzisoxazole-3-methane sulfonic acid (BOS-NH4), which can be crystalline. The present invention also provides substantially chemically pure BOS-NH4, which is non- hygroscopic or slightly hygroscopic. Another aspect of the present invention is directed to processes of preparing the BOS-NH4. The present invention also provides processes for preparing l,2-benzisoxazole-3-methane-sulfonyl chloride (BOS-Cl) using the BOS-NH4. The present invention also provides processes for preparing zonisamide using the BOS-NH4 or BOS-Cl.
US20110104162 Compounds which can be used for the Treatment of Cancers The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
CA2293358C Tricyclic sulfonamide inhibitors of farnesyl-protein transferase Novel tricyclic sulfonamide compounds of formula (1.0) and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel sulfonamide compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
EP2130533A1 Ataractic agent and functional food This invention provides a pharmaceutical and functional food which are made of a safe food ingredient or nutrient which has been used for a long period of time, and which have tranquilizing effect such as anti-anxiety effect, anti-depression effect, and anti-stress effect. The tranquilizer of the invention contains vitamin K as an active ingredient. Vitamin K is preferably menaquinone-4 and/or menaquinone-7. This invention also provides a supplement, health food or functional food for tranquilizing purpose that contains vitamin K as an active ingredient.
CA2321909C Product and method to reduce stress induced immune suppression In its broadest aspect, the present invention is directed to the discovery of immunonutritional products that are useful in reducing the immunological system suppression that results from stress. The stress may be in the form of physical exertion, mental exhaustion, disease states and the like. In one embodiment, the invention relates to a nutritional composition comprising a structured glyceride component and an antioxidant system. This nutritional composition has been shown to be highly effective in reducing immune system down regulation or dysregulation as a result of stress.
WO2012013848A1 Difluorobenzyl ethanolamine derivatives with antimicrobial activity Difluorobenzyl ethanolamine derivatives with antimicrobial activity, belonging to the field of chemistry/medicine. Reference is made to a method for synthesizing fluorinated ethanolamine molecules, specifically difluorobenzyl ethanolamines, and also to said novel molecules and to the activity thereof that inhibits the growth of species of the genera Mycobacterium and Nocardia, which are pathogenic bacteria involved in the development of diseases such as tuberculosis or leprosy, and also other pulmonary, cutaneous or central-nervous-system infections.
EP2451280A1 Method of wound healing and scar modulation The invention relates to methods of promoting wound healing and reducing scar formation by administration of corticosteroids, and pharmaceutical compositions comprising corticosteroids.
US20080045477 Series Of New 4,6-Diamino-1,2-Dihydro-1-Aryl-1,3,5-Triazines, Substituted By An Adamantyl Moiety In The Position 2 Of Triazine-Their Corresponding Salts, Isomers,Steroisomers, Enantiomers, Free Bases And The Complexes Of All The Above With Natural Macromolecules And Their Synthetic Derivatives. A series of new 4,6-diamino-1,2-dihydro-1-aryl-2-(-tricyclo[3.3.1.13,7]decyl]-1,3,5-triazines where the aryl group is a substituted or unsubstituted phenyl, or naphthyl-group, as pharmaceutically accepted salts or as free bases. The phenyl group substituents are halides, alkyls, alkoxyls or nitro group. One or more of the above substituents are found one or more times each one, and in various positions of the phenyl group. The corresponding isomers, stereoisomers, enantiomers, free bases and their complexes with various natural macromolecules and synthetic derivatives of them. The invention refers to new and prototype compounds inhibiting the proliferation of unwanted cells that belong to pathogenic microorganisms, to human tissues, to pathological cells, or any pathological cell proliferation. It also refers to the synthesis and the method of synthesis of the above mentioned compounds. The synthesis and the method of synthesis thereof of a series characterized by the preparation of the final triazines, by cyclization of the bigouanide hydrochlorides with adamantane-1-carboxaldehyde. Preparation of the inclusion complexes is realized from compexation of the corresponding hydrochlorides of the above mentioned triazines with natural macromolecules or synthetic derivatives.
EP2546249A1 5-Alkynyl-pyridines This invention relates to 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity ofPI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.
US20120141371 Antibody compositions, methods for treating neoplastic disease and methods for regulating fertility Antibody compositions and methods for inhibition of the effects of gonadotropin hormones are provided. Methods for treating cancer and methods for regulating fertility are provided by administration of the antibody compositions to a mammalian subject in need thereof.
US8685473 Pawpaw and/or peach derived composition There is provided a process for making a composition suitable for topical application comprising the steps of a) heating at least one fruit and/or vegetable pulp to up to a temperature in the range of about 40° C. to 100° C.; b) mixing between 1 and 40% w/w of a mild base with the heated fruit and/or vegetable pulp. There is also provided a fruit and/or vegetable derived composition suitable for topical application prepared by the above process. There is further provided a fruit and/or vegetable derived composition comprising at least one fruit and/or vegetable derived pulp and a mild base, said composition having a pH in the range of about 7.5 to about 9.5.
WO2014085866A1 USE OF miRNA ANTAGONISTS FOR IMMUNE SYSTEM MODULATION, TREATMENT OF BACTERIAL INFECTIONS AND TREATMENT OF AIRWAYS DISEASES Disclosed herein are immunostimulatory compositions comprising at least one agent capable of inhibiting the expression and/or activity of miR-328-3p, a precursor or variant thereof or a miRNA comprising a seed region comprising the sequence UGGCCCU. Also disclosed herein are uses of said compositions for, inter alia, treating bacterial infections, promoting bacterial clearance, treating airways diseases and treating immunodeficiency.
CN1597674A 1, 3-di[N-(2-methoxy) phenyl] piperazine]-1- acetone hydrochloride and its preparation method and application A 1,3-bis[N-[N-(2-methoxy)phenyl]piperazinyl]-1-acetone hydrochloride, its preparing process, and its application in preparing medicine for treating blood cancer are disclosed.
CN103610674A Solid preparation containing micronized prasugrel The invention relates to a solid preparation containing micronized prasugrel. The prasugrel is micronized by adopting a superfine grinding technology, and then the solid preparation is prepared from a medicinal additive applicable to preparation of the prasugrel solid preparation, wherein the prasugrel accounts for 0.1-30% of total weight. The micronized prasugrel compound is prepared by adopting the superfine grinding technology, so that the water solubility of the prasugrel is improved, the bioavailability is improved, and the clinical effect of the drug preparation is increased.
US8173156 Method for avoiding crystallization of anti-inflammatory agent in plaster formulation An anti-inflammatory-containing plaster is provided. The anti-inflammatory-containing plaster may include, e.g., a styrene-isoprene-styrene block copolymer, a high molecular weight polyisobutylene, a low molecular weight polyisobutylene, a tackifier, a plasticizer, a dispersant, and an anti-inflammatory having a carboxyl group or a salt thereof. However, the anti-inflammatory-containing plaster does not contain L-menthol. The anti-inflammatory-containing plaster has medicament release rates of 20-64% by mass and 40-93% by mass at one hour and three hours, respectively.
CA2549303A1 Novel sodium channel Novel sodium channel nucleic acids and polypeptides are disclosed herein. Methods of using the novel nucleic acids and polypeptides are also disclosed.
CN102488696A Glycerin-fructose composition injection and its preparation method The invention relates to a glycerin-fructose composition injection and its preparation method. The composition contains glycerin, fructose, mannitol and sodium chloride. By the adoption of the method, the problem of poor stability of present glycerin-fructose injections is effectively solved, and stability and drug use safety of the preparation are raised. In addition, by the combination of glycerin, fructose and mannitol, the problem that a mannitol preparation is easy to crystallize can be effectively solved, and the damage to the kidney can be also mitigated.
EP2246054A1 Fentanyl-containing patch for external use A patch for external use which has a laminate structure comprising a substrate and a pressure-sensitive adhesive layer which contains a styrene/isoprene/styrene block copolymer as the base and further contains a tackifier resin consisting of a rosin resin and at least one other tackifier resin, a softening agent consisting of polybutene and liquid paraffin, a fatty acid ester, and fentanyl, characterized in that the weight ratio of the rosin resin to fentanyl is 1 to 5, the weight ratio of the rosin resin to the whole tackifier resin is 0.1 to 0.6, and the tackifier resin accounts for 30 to 60wt% of the whole pressure-sensitive adhesive layer. The patch is excellent in the permeation of fentanyl through the skin and in storage stability, and is weak in irritation to skin.
EP1113795B1 Tryptophanyl esters and their n-acyl derivatives for the prevention and treatment of diseases caused or exacerbated by oxidation processes The invention relates to the use of a tryptophanyl ester or an N-acyl derivative of a tryptophanyl ester for the prophylaxis and treatment of oxidative pathological processes in degenerative diseases and/or carcinomas. The tryptophanyl ester or its N-acyl derivative are preferably tryptophanoctyl ester, N-oleol-tryptophan ethyl ester or N-dodecanoyl-tryptophan ethyl ester. Furthermore, the tryptophanyl esters and their N-acyl derivatives are preferably used for the treatment and/or prophylaxis of neurodegenerative diseases, cataracts, neoplastic diseases and/or cardiovascular diseases. The invention notably relates to the use of the tryptophanyl esters and their N-acyl derivatives for the treatment and/or prevention of Alzheimer's disease, Parkinson disease, stroke, amyotrophic lateral sclerosis, cancer, arteriosclerosis and/or myocardial infarction. The invention further relates to a medicament containing a tryptophanyl ester or an N-acyl derivative of a tryptophanyl ester.
US20120087957 Process for the preparation of pharmaceutical suspensions for inhalation Process for preparing sterile suspensions for inhalation comprising an active ingredient insoluble in water and wherein at least 80% of the particles of said active ingredient have a diameter between 3 and 5 μm, comprising the following stages: dissolving the active ingredient in the minimum quantity of an alcoholic solvent, optionally in the presence of a polyol and adding at least one surfactant, filtering the solution obtained in the previous stage through a sterilizing filter, adding the solution from stage (b) to sterile water under sonication to directly obtain a suspension wherein the particles have a reduced diameter.
CN102160860A Medicament for promoting hair growth and preventing hair loss and preparation method thereof The invention discloses a medicament for promoting hair growth and preventing hair loss. The medicament comprises the following components in percentage by weight: 50-95% of acid-resistant substrate used as a solvent and 5-50% of hydroxy acid used as a solute. The invention also discloses a method for preparing the medicament for promoting hair growth and preventing hair loss. The method comprises the following steps of: preparing the acid-resistant substrate used as the solvent; and adding the hydroxy acid used as the solute according to the concentration of 10-25%. The medicament for promoting hair growth and preventing hair loss achieves the effects on preventing hair loss and promoting hair growth by improving the skin quality and subdermal vascular plexus; the effect duration time is long, and the side effects of the existing like products are avoided; and the medicament can be better used for treating hair loss and promoting hair growth.
WO2005001469A1 Method of acidic polysaccharide analysis and kit for the analysis A method of acidic polysaccharide analysis that can not only realize a high-speed analysis but also find the possibility of high-sensitivity analysis; and a kit for use in the effectuation of the analytical method. Pretreatments having been needed for fluorescent labeling can be avoided by using the phenomenon that acidic polysaccharides form a complex in cooperation with a quaternary ammonium salt (e.g., ethidium bromide or propydium iodide) to thereby induce fluorescent emission and by carrying out electrophoresis with the use of a buffer for electrophoresis containing a quaternary ammonium salt. Moreover, an about 60-fold reduction of analytical time as compared with that of conventional methods can be achieved by the application of a microchip electrophoresis method having been developed in recent years in order to attain high-speed analysis of DNA.
CN103301116A Oral medical composition The invention provides a 5-[1, 2-Dihydro-2-oxo-3H-indol-3-ylidene) methyl]-2, 4-dimethyl-1H-pyrrole-3-propanoic acid (TSU-68)-containing oral medical composition which has quick dissolution performance and still has slightly reduced dissolution performance after long-term storage. The oral administration medical composition comprises 3-(2, 4-dimethyl-5-{[(3Z)-2-oxo-1, 2-dihydro-3H-indole-3-subunit] methyl}-1H-pyrrole-3-radical) propanoic acid as an effective ingredient, does not contain an adhesive in nature and contains a specific amount of carboxymethyl cellulose as a disintegrating agent.
EP2303252A1 Compounds for the treatment of metabolic syndrome and insulin resistance The present invention provides a compound comprising an ellagic acid moiety, such as ellagic acid itself, ellagitannins and ellagic acid glycosides - as well as plant extracts comprising the same, for the treatment or prevention of Metabolic Syndrome or non-diabetic insulin resistance.
CN1875977A Use of tanshinone compound in preparation of medicine for treating Grave's disease The invention discloses the use of tanshinone compounds in preparing medicaments for treating Graves diease. Plenty of animal and human body tests shows that, tanshinone compounds have evident actions for treating and improving Graves diease.
CN103372131A Immersion liquid conducive to treatment of dermatophytosis, tinea pedis, foot odor and helosis The invention relates to immersion liquid conducive to treatment of dermatophytosis, tinea pedis, foot odor and helosis. The preparation method mainly comprises the following steps: firstly, selecting a glass jar to sterilize, taking 2 parts of white vinegar and 1 part of garlic to pour into the jar to mix according to the parts by weight; then taking 0.05 parts of white spirit to pour into the glass jar to seal; keeping in shade and fertilizing for half a year to prepare yellow liquid. The immersion liquid has the beneficial effects that the immersion liquid has the advantages of being convenient to use, low in cost, free of damage to skin and the like, adopts an immersion mode, and has good effects of sterilizing and disinfecting. By using the immersion liquid prepared by the method, a sufferer soaks hands, feet and the parts with the disease states, for example, callus peeling, dermatophytosis, foot odor, helosis and the like into the liquid for 20 minutes; the immersion liquid is used for once or twice in every day and a week is taken as a treatment course; the situation that the disease states are improved or cured after a plurality of treatment courses is contributed.
CN1657044A Chlorretadin oral disintegrating tablet and its preparation method An oral disintegrating tablet of loratadine for treating allergic rhinitis, urticaria and other allergic skin diseases is prepared from loratadine and medicinal auxiliary.
CN102648912A New use of 4-amino piperidines compound The invention belongs to the field of medicine and relates to a new use of 4-amino piperidines compound. Particularly, the invention relates to a use of 4-amino piperidines compound shown in the formula I or the medicinal salt of 4-amino piperidines compound in preparation of medicine for treatment or adjuvant therapy of tumours, a use in preparation of medicine or agents for blocking or restraining a potassium channel, a use in preparation of medicine or agents for blocking or restraining current of a potassium channel, and a use in preparation of medicine or agents for restraining SH-SY5Y cells.
CN101269014A Orally disintegrating tablet of risperidone and preparation method thereof The invention discloses an orally disintegrating tablet containing risperidone and a preparation method thereof. The orally disintegrating tablet contains solid dispersing carrier material and other accessory materials which is acceptable in pharmacy, adopts the solid dispersing technology to effectively hide the taste and is prepared by using a powder pressed disc method or pellet fabrication pressed disc method; the orally disintegrating tablet has the advantages of good mouthfeel and convenient taking, and is used for curing acute or chronic psychosis.
US20090118305 Pyridine and pyrazine derivatives - 083 The invention concerns pyridine and pyrazine derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of W, G1, G2, G3, G4, J, Ring A, n and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
WO2014050779A1 Combination of gsk3 inhibitor and anti-dr5 antibody To provide a combination therapy for cancer, which comprises a combination of a GSK3 inhibitor and an anti-DR5 antibody. Provided are a pharmaceutical product and a combination therapy, each of which comprises a combination of various anti-DR5 antibodies and a GSK3 inhibitor such as LY2090314, a compound represented by general formula (1) or a salt of the compound. (In the formula, R1, R2, R3, R4, X1 and X2 are as defined in the description.)
CA2189778C Use of fas ligand to suppress lymphocyte-mediated immune responses Soluble mouse and human Fas ligand polypeptides and methods for inhibitng T-lymphocyte-mediated immune responses, including those directed against autologous and/or heterologous tissues, e g., by a recipient mammal of a transplanted tissue, by providing the recipient mammal with Fas ligand. The Fas ligand may be provided to the recipient mammal by a variety of means,including by direct administration of the Fas ligand or by providing the gene encoding the Fas ligand to a subject such that Fas ligand is synthesized by the subject.
US20060058398 Medicinal compositions containing vitamin k's as nerve growth factor potentiator and utilization thereof To provide medicinal compositions containing an active ingredient which has a low molecular weight, is free from any side effects and has an effect of potentiating nerve growth factor activity and utilization thereof for treating diseases associated with dementia, medicinal preparations containing an effective amount of vitamin K and/or its derivative showing an effect of potentiating nerve growth factor activity are provided.
CN1593428A Dextran-aspirin combined medicine and its preparation method The invention discloses a dextran-aspirin combined medicine and its preparation method, wherein the medicament has the structural formula disclosed in the specification, n=120-250. The medicament can reduce the side effects to stomach and intestine, and extend the internal release time.
CN102908358A Compound preparation for preventing and treating proventriculitis of chicken The invention belongs to a chicken proventriculitis preventing and treating composition of veterinary medicines. The chicken proventriculitis preventing and treating composition is obtained by compounding amoxicillin, cimetidine, aspirin, metoclopramide, baking soda and the like. The weight ratio of each active ingredient is as follows: 10% of amoxicillin, 5% of cimetidine, 10% of aspirin, 0.1% of metoclopramide, 15% of baking soda and the balance of glucose. The veterinary medicine composition is used for treating proventriculitis diseases of chicken. A processing process of the composition comprises the steps of respectively crushing and screening each ingredient, accurately weighing each ingredient according to the desired ratio, mixing the ingredients for 25 min, inspecting the qualities of semi-finished products, separately filling the semi-finished products, packaging the semi-finished products and inspecting the qualities of finished products. A use method comprises the steps of drinking water mixed with 1% of the composition and continuously drinking the water for a treatment course of 3-5 days. The chicken proventriculitis preventing and treating composition provided by the invention has the advantages of high sensitivity to chicken proventriculitis, obvious effect, low drug resistance, convenience in use and very good promotion and application values.
DE102005026051A1 Mixture, useful in photodynamic therapy as photosensitizer and/or fluorescence active substance, comprises chlorin e6 derivatives and pyrrolidone derivatives Mixture comprises chlorin e6 and/or its derivatives (I) and pyrrolidone derivatives (II). Mixture comprises chlorin e6 and/or its derivatives of formula (I) and pyrrolidone derivatives of formula (II). M : bivalent metal ion or two H, each of which is bound to one of the N atoms; M1>H or metallic cation; and R : optionally substituted alkyl group with 1-12 or more C atoms. [Image] - ACTIVITY : Dermatological; Fungicide; Antipsoriatic; Antiseborrheic; Ophthalmological. - MECHANISM OF ACTION : None given.
CN102429900A Application of natural compound P25 in inhibiting reproduction and growth of tumour cells The invention discloses an application of natural compound P25 in inhibiting activation of reproduction and growth of tumour cells. The structure formula of the natural compound P25 is showed in formula I. The compound or the pharmaceutically acceptable salt thereof can be used for preparing the drugs for inhibiting the propagation of the tumour cells of the eucaryon or the drugs for preventing and/or treating the tumours. The in-vitro anti-tumour experiment proves that the compound P25 has better inhibiting effects on breast cancer cells (MCF-7), lung cancer cells (A549), colon cancer cells (Caco2, SW480) and vero fibrocyte (COS-7).
CN101032470A Povidone-iodine bubble agent and preparing method The present invention is polyvidone iodine foam agent and its preparation process. The process of preparing polyvidone iodine foam agent includes the steps of: dissolving polyvidone iodine in water; adding span-80, sodium dodecyl sulfate, glycerin, etc via homogeneous mixing; adding distilled water via stirring and regulating pH value; filling the mixture into container, setting in emulsion pump and pressing the emulsion pump manually to generate foam. The foam agent makes its medicine distributed inside vagina or on the surface of skin to take action fast. The foam agent has fast and high treating effect, high safety and use convenience, and is one good medicine for treating gynecologic diseases.
WO2008137137A1 Creatine ascorbyl derivatives and methods of use thereof The present invention provides methods of treating creatine responsive states, such as a neurological disorder (i.e. , Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, muscular dystrophy, Charcot Marie Tooth syndrome, Alzheimer's disease, or creatine transporter defect) or a skin disorder, by administering a creatine-ascorbyl derivative.
WO2014071231A1 Tec family kinase inhibitor adjuvant therapy Described herein are methods and compositions comprising a covalent TEC family kinase inhibitor for use in adjuvant therapy, including adjuvant cancer therapy, vaccination and treatment of immune disorders and pathogenic infections.
CN103462973A Application of Incarviatone A in medicaments for treating lung cancer The invention discloses an application of Incarviatone A in preparation of medicaments for treating lung cancer. The compound shows good anti-lung cancer activity, can be used for preparing anti-lung cancer medicaments, and belongs to the technical field of a new application of medicaments. The Incarviatone A can prominently inhibit non-small cell lung cancer cells A549, large cell lung cancer cells NCI-H460, lung squamous cells HTB-8 and human lung flat epithelial cancer cells QG-5 cultured in vitro, has a low inhibiting effect on human normal liver cells LO2 and peripheral blood lymphocytes, and shows obvious selectivity. The application of the Incarviatone A in preparation of the medicaments for treating the lung cancer is made public for the first time, the skeleton type is completely novel, and the Incarviatone A has an unexpectedly strong lung cancer cell inhibiting activity.
CA2399840C Use of roflumilast or pumafentrine in combination with methotrexate for the treatment of arthritic diseases The invention relates to the combined administration of a PDE4 or PDE3/4 inhibitor and a disease modifying anti-rheumatic drug (DMARDs) or anti-rheumatic or anti-arthritic drug.
CN103284977A Diarrhea paste for infants The invention discloses a diarrhea paste for infants. The diarrhea paste comprises a substrate, wherein a non-woven fabric is arranged on the outer layer of the substrate, and ceramic micropowder is arranged at the inner layer of the substrate. The diarrhea paste adopts a paste structure, is convenient to use without causing anaphylaxis and medicine loss and contaminating clothes, and can be used for curing the diarrhea within short time.
US7271165 Useful for treating or preventing a variety of antibiotic resistant microbial infections; for example, 25-O-deacetyl-25-(2'',3''-dihydroxypropylcarbonoxy)-5'-[4-isobutyl-1-piperazinyl]benzoxazinorifamycin The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.
US8119638 Compositions and uses of ET743 for treating cancer Et 743 is used in the preparation of a medicament for the treatment of the human body for cancer.
US20100093841 Cell culture system of a hepatitis c genotype 3a and 2a chimera The present inventors have developed a culture system for genotype 3a, which has a high prevalence worldwide. Since intergenotypic recombinant genomes exploiting the replication characteristics of JFH1 will be a valuable tool for the genotype specific study of the replaced genes and related therapeutics, the present inventors constructed a genotype 3a/2a (S52/JFH1) recombinant containing the structural genes (Core, E1, E2), p7 and NS2 of strain S52 and characterized it in Huh7.5 cells. S52/JFH1 and J6/JFH viruses passaged in cell culture had comparable growth kinetics and yielded similar peak HCV RNA titers and infectivity titers. Direct genome sequencing of cell culture derived S52/JFH1 viruses identified putative adaptive mutations in Core, E2, p7, NS3 and NS5A; clonal analysis revealed, that all genomes analyzed exhibited different combinations of these mutations. Finally, viruses resulting from transfection with RNA transcripts of five S52/JFH1 recombinant containing these combinations of putative adaptive mutations performed as efficiently as J6/JFH viruses in Huh7.5 15 cells and were all genetically stable after viral passage. In conclusion, the present inventors have developed a robust and genetically stable cell culture system for HCV genotype 3a.
US20120295858 Use of danshensu, notoginsenoside r1 or their combination in preparation of medicaments for preventing and treating diseases caused by microcirculation disorder The present invention relates to a new use of traditional Chinese drug products of Danshensu (DLA), Notoginsenoside R1 (R1) and their combination, in particular to the therapeutic and preventive effects of DLA, R1 and their combination on the diseases caused by microcirculation disorder.
EP0944639A4 Synthetic glycoamines, methods for their use that affect cell A class of molecules and methods that alter cell adhesion, inhibit cancer metastasis, and induce apoptosis. A method according to the present invention comprises bringing cells into contact with compounds that essentially consist of an amino acid linked to a carbohydrate wherein the amino acid and the carbohydrate are linked to form a compound chosen from the group consisting of Schiff bases, N-glycosides, esters, and Amadori products. The carbohydrate is preferably a monosaccharide or a small digosaccharide. The carbohydrate and amino acid sub-units may be chemically modified. For example, the amino acid may be modified by covalently bonding other groups to the amino group, carboxyl group, or side chain group of the amino acid. The carbohydrate sub-unit is preferably a pentose such as arabinose, xylose, ribose, ribulose, a hexose such as fructose, deoxyfructose, galactose, glucose, mannose, tagatose, rhamnose, or a disaccharide based on two of the above such as maltose, lactose, maltulose, or lactulose.
WO2009070516A1 Imidazo-thiazole derivatives as protein kinase inhibitors Compounds of formula I that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed. Formula I and therapeutically acceptable salts, prodrugs and salts of prodrugs thereof, wherein X is CH or N; A1 is R1, OR1. NHR1, N(R1)2, NHC(O)R1, NHC(O)NHR1, NHC(O)N(R1)2, NHC(O)OR1, C(O)NHR1, C(O)N(R1)2, C=NOR1, or C(NH2)NOC(O)R1;
CA2779009A1 Novel antitumoral use of cabazitaxel The invention relates to a compound of Formula (I): which may be in base form or in the form of a hydrate or a solvate, in combination with prednisone or prednisolone, for its use as a medicament in the treatment of prostate cancer, particularly metastatic prostate cancer, especially for patients who are not catered for by a taxane-based treatment.
US20060140906 Composition comprising cysteamine for improving immunity of animals There is provided a new use of cysteamine, a salt thereof, or a composition containing cysteamine or a salt thereof, for improving immunity of animals.
CN102989011A Medicine composition for treating liver caner and application thereof The invention discloses a medicine composition for treating liver caner and application thereof. The medicine composition is a medicine composition containing arsenic trioxide and recombinant adenovirus containing PML (promyelocytic leukemia protein) gene for jointly treating liver cancer, and belongs to the field of biological medicines. According to the medicine composition, the therapy idea of arsenic trioxide and PML gene recombinant adenovirus for jointly treating liver cancer is put forward for the first time; the effect of in vitro and in vivo treating liver cancer by jointly applying arsenic trioxide and PML gene recombinant adenovirus is observed and the action mechanism and characteristics are disclosed through the exertion of molecular biology and cellular biological technology; and the medicine composition provides a theoretical basis and a new method for treating liver cancer.
CN102406628A Method for preparing stable esomeprazole enteric-coated pills The invention provides a method for preparing stable esomeprazole enteric-coated pills, which comprises: (1) preparing pill cores containing a medicine and controlling the free water in the pill cores containing the medicine to be less than 2.5 weight percent; and (2) performing enteric coating under a condition that the free water content in the pill cores containing the medicine is controlled to be less than 2.5 weight percent. The invention provides a new feasible process method for replacing an isolating layer, thereby overcoming the complexity of a preparation process and adverse effect on enteric-coated medicine disintegration, exsolution or the like in the prior art.
US7601343 An isolated RNA-pulsed antigen presenting cell comprising tumor specific RNA; stimulation of cytotoxic T-lymphocyte proliferation ex vivo or in vivo for adoptive immunotherapy; anticarcinogenic agents; antitumor agents; bactericides; viricides Disclosed are cells and methods for treating or preventing tumor formation or infections with pathogens in a patient. The cells of the invention are antigen-presenting cells (e.g., dendritic cells or macrophage) that have been loaded with RNA derived from tumors or pathogens. By administering the RNA-loaded antigen-presenting cells to a patient, tumor formation or pathogen infections can be treated or prevented. Alternatively, the RNA-loaded cells can be used as stimulator cells in the ex vivo expansion of CTL. Such CTL can then be used in a variation of conventional adoptive immunotherapy techniques.
CN103040852A Application of lysine as synergist for preparing antifungal drug The invention relates to the medical technology field, and discloses an application of lysine as a synergist for preparing antifungal drugs like polyenes or echinocandins. The antifungal drugs may be amphotericin B, nystatin or caspofungin. The amount of lysine or pharmaceutically acceptable salts thereof in the antifungal drug effective concentration is 0.03-0.5mM. As shown in an experiment, the combination application of antifungal drugs like amphotericin B, nystatin and caspofungin, can also ensure the treatment effect on superficial and deep fungal infections in case of decrease of drug dose, and the combination can be used as a synergist of the antifungal drugs. The lysine, as the synergist of the antifungal drugs, can decrease the medical dosage of the antifungal drugs like polyenes or echinocandins, thereby alleviating the toxic and side effect of medicaments, effectively treating fungal infection, and having a high application value.
CA2305394C Local administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction A method is provided for treating erectile dysfunction in a mammalian male individual. The method involves the local administration of a phosphodiesterase inhibitor or a pharmaceutically acceptable salt, ester, amide or derivative thereof, within the context of an effective dosing regimen. A preferred mode of administration is transurethral. Pharmaceutical formulations and kits are provided as well.
EP1689717B1 Substituted isoquinolines useful in the treatment of diseases such as cancer and atherosclerosis A compound of Formula (I) wherein: One of R1 and R2 is H and the other represents - NHCONHR4 wherein R4 represents a phenyl or naphthyl group (which may be optionally substituted by one or more substituents independently selected from -C1-6 alkyl, -C1-6 haloalkyl, - CH2CH2CH2-, halogen, C1-6 alkoxy, C1-6 haloalkoxy, OH, NO2), C3-7 cycloalkyl or R4 together with the NH to which it is bonded forms a morpholino group and R3 is H or NHR5 wherein R5 is H, -quinolinyl or -isoquinolinyl, -(CONH)p phenyl (wherein p is 0 or 1 and the phenyl is optionally substituted by one or more substituents independently selected from halogen, -C1-6 alkyl, -C1-6 haloalkyl, -morpholino, -SO2NH2, benzothiazole (substituted by methyl)) or a salt, solvate, or physiologically functional derivative thereof.
CN103169656A Cucurbitacin oral lipid nano emulsion and preparation method The invention discloses a prescription for preparing a cucurbitacin oral lipid nano emulsion and a preparation method. The cucurbitacin oral lipid nano emulsion contains cucurbitacin, medium chain triglyceride, soya lecithin, polyoxyethylene 40 hydrogenated castor oil, an antifreezing agent, vitamin E and water. The prepared cucurbitacin oral lipid nano emulsion has good antifreezing capability, Compared with the tablet in the market, the disintegration of the tablet in the gastrointestinal tract is not existed, the dissolution of the medicine is fast, the cucurbitacin oral lipid nano emulsion is widely and uniformly distributed in a easy mode, the acting time is fast, and the bioavailability of the cucurbitacin oral lipid nano emulsion is obviously enhanced. The preparation technology is simple, and can be used for industrial production.
CN102239170A Substituted tetrahydropyran spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I) Wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
CN102068429A Application of fadrozole in inducing transformation of differentiated ovary of tilapia mossambica into functional testis and induction method thereof The invention belongs to the technical field of inheritance breeding of fishes and relates to the application of fadrozole in inducing the transformation of the differentiated ovary of tilapia mossambica into functional testis and a method for inducting the transformation of the differentiated ovary of tilapia mossambica into the functional testis. In the method, a fadrozole-containing bait is continuously fed to female tilapia mossambica of which the sex gland has been differentiated into an ovary until the ovary is transformed into the functional testis. Fadrozole serving as an aromatase inhibitor is used for inducing the transformation of the differentiated ovary of tilapia mossambica into the functional testis, so that re-differentiation of the differentiated ovaries of all vertebrates into the functional testis is realized through a manual factor apart from natural reversed types, a new method for inducing the reversion of tilapia mossambica from a female individual into a male individual is established, a reliable experiment model is provided for researches on the molecular mechanism of the determination and differentiation of the gender of tilapia mossambica, and a new technical measure for the gender control of tilapia mossambica and single-gender breeding is established.
EP1551369A2 Combination therapy for treatment of fibrotic disorders The present invention provides methods of treating a fibrotic disorder. The methods generally involve administering an effective amount of IFN-γ and an effective amount of pirfenidone or a pirfenidone analog.
US20090036450 Pyrazole compounds and use thereof The pyrazole compound of the present invention is represented by the following general formula (I). The pyrazole compound of the present invention or a salt thereof or a solvate thereof potently inhibits liver glycogen phosphorylase, and, therefore, is useful as a therapeutic or prophylactic agent for diabetes. wherein each symbol denotes as described in the specifications.
CA2315685C Molecular dispersion composition with enhanced bioavailability A molecular dispersion composition is disclosed. The molecular dispersion comprises a compound of formula (1) molecularly dispersed in a polymer matrix. Also disclosed are solid dosage forms, e.g., tablets and capsules, containing these molecular dispersions.
US20120238937 Method of treating keloids or hypertrophic scars using antisense compounds targeting connective tissue growth factor (ctgf) This invention provides methods of preventing formation of, or treating, fibrotic lesions, including skin scars such as keloids and hypertrophic scars which comprise administering to the subject by one or more injection a compound which comprises a modified oligonucleotide, such as a modified antisense oligonucleotide, siRNA, or oligodeoxyribonucleotide, which inhibits expression of protein involved in fibrosis. Dosing of the antisense using an intradermal threading technique is also described.
USRE38912 for treating a number of complaints, particularly respiratory diseases The invention relates to a new process for producing powdered preparations for inhalation.
WO2010022461A1 Sulphated sugars to increase activity of sulphatases en lysosomal storage disorders A method an preparation for increasing the activity of a sulphatase associated with a lysosomal storage disorder comprising administering a sulphated sugar. In particular useful for the lysosomal storage disorders associated with the following sulphatases:-iduronate-2-sulphatase, sulphamidase, glucosamine 6-sulphatase, galactose 6-sulphatase, galactosamine 4-sulphatase and galactose 3-sulphatase. The sulphated sugar is proposed to act as a pharmaceutical chaperone stabilizing the nascent sulphatase at the higher pH levels encountered in the endoplasmic reticulum (ER) and during transportation of the nascent sulphatase from the ER to the lysosome thereby avoiding the endoplasmic reticulum- associated degradation system. The sulphated sugar is preferably a monosaccharide thus not acting as a substrate and is released at the lower lysosomal pH levels where at least some activity is exhibited.
EP2776044A1 Pharmaceutical compositions comprising lubricants for preventing or reducing aseptic loosening in a subject The present invention relates to pharmaceutical compositions comprising one or more amphiphilic polymer lubricants for use in association with artificial orthopaedic implants. Additionally, the invention relates to medical use of the lubricants of the invention in connection with conditions associated with artificial5 orthopaedic implants. The invention furthermore relates to artificial joint implants comprising the polymer lubricants according to the invention and methods for preparing such implants.
US20100105685 S-Nitrosothiol Compounds and Related Derivatives The present invention is directed to a method of treating a lack of normal breathing control including the treatment of apnea and hypoventilation associated with sleep, obesity, certain medicines and other medical conditions. In an aspect, the invention is directed to treating disordered control of breathing by administering an composition comprising a single compound which treats lack of normal breathing. In another aspect, the invention is directed to treating disordered control of breathing by administering an composition comprising a combination of two or more compounds, at least one of which treats lack of normal breathing. In an aspect, a compound is an S-nitrosylating agent.
CN102989002A DOX-P micelle with anti-tumor drug resistance and preparation method thereof The invention discloses poloxamer-adriamycin conjugate (DOX-P) micelle with anti-tumor drug resistance and a preparation method of the DOX-P micelle. The synthetic process of the DOX-P comprises the steps of firstly, reacting poloxamer with succinic anhydride to obtain high-molecular polymer of which the tail end contains carboxyl; and then, directly bonding the carboxyl at the tail end of the polymer with primaquine group in the adriamycin in an amido bond mode. The DOX-P has the capability of forming the micelle; and compared with the adriamycin bulk drug, the adriamycin subjected to covalent binding in the DOX-P micelle has the advantages that the anti-tumor activity of the adriamycin is maintained, the drug resistance of the tumor is overcome, and the stability of the adriamycin is better than that of poloxamer micelle.
WO2009117985A1 Pirinixic acid derivatives as prostglandin e2 synthesis inhibitors for treating inflammatory diseases The invention relates to pirinixic acid derivatives, especially α-substituted pirinixic acids and pirinixic acid esters, and the structural derivatives thereof with the following structural formula. The pirinixic acid derivatives inhibit the PGE2 synthesis, especially that of the mPGES-1. The invention also relates to the use of said pirinixic acid derivatives for producing a medicament for treating prostaglandin E2-mediated diseases, especially inflammatory diseases, painful and feverish conditions, cardiovascular events and cancerous diseases associated with an increased inducible microsomal prostaglandin E2 synthesis-1 (mPGES-1) activity or increased prostaglandin E2 synthesis.
CA2370202C Gum pad for delivery of medication to mucosal tissues The gum pad (10) is a laminate composed of: (a) a synthetic base or backing layer (12) which is configured to be held in place on the gingiva (gums) in the mouth; (b) an intermediate reservoir layer (14) for containing medication (16) therein; and (c) a semi-permeable outer layer (18) facing outwardly towards the oral mucosal tissue (22) in the mouth which will allow saliva to enter and dissolve the medication in the reservoir layer (14) into solution and pass the diffused saliva-medication solution out-wardly to the oral mucosal tissue (22). The backing layer is placed on the gum so that the semi-permeable outer layer (18) faces outwardly toward the buccal mucosa (22). Saliva enters the semi-permeable layer (18) and dissolves the medication in the reservoir layer (14), then diffuses outwardly through the semi-permeable layer (18) to the mucosal tissue in the mouth where it is readily absorbed into the circulatory system. The gum pad (10) can be used for the topical or systemic delivery of a wide range of pharmaceutical and nutritional agents, for the treatment of a variety of human disorders and diseases.
US20110275715 Method for treating retinal disease The present application provides a method for treating a retinal disease in a patient in need thereof, which comprises administering at least three drops of an ophthalmic composition comprising a fatty acid derivative as an active ingredient in an eye of the patient per day.
EP2581451A1 Compounds for inhibiting mammalian s-nitrosoglutathione reductase The current study reports novel inhibitors of s-nitrosoglutathione reductase (GSNOR) identified that specifically inhibit GSNOR among the alcohol dehydrogenases. These inhibitors may bind into the GSNO binding site and inhibit GSNOR at multiple places in its kinetic pathway. These molecules inhibit GSNOR in a dose dependent manner and demonstrate that GSNOR actively regulates the s-nitrosylation of proteins against incoming low molecular weight nitrosothiols. These compounds are useful in method of treatment of diseases such as asthma, chronic obstructive pulmonary disease, heart disease, heart failure, heart attack, hypertension, atherosclerosis, restenosis, impotence, Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, stroke, septic shock, cardiogenic shock, endotoxic shock, toxic shock syndrome, systemic inflammatory response syndrome, and other inflammatory diseases. These compounds can also be used to diagnose and/or study disease and/or conditions or enzymes involving the s-nitrosylation of proteins.
WO2012062031A1 Drink of nourishing lung A functional drink made by pinecone, fresh pear pericarp and other raw materials, having an effect of nourishing lung is provided.
CN1727351A Method for preparing compound of vegetative phosphatidylinositol in high purity A process for preparing the high-purity (more than 96%) vegetative phosphatidylinositol (PI) from soybean includes such steps as extracting in solvent, separating, and purifying by macroreticular resin chromatography. Said PI has high activity of selectively killing more kinds of human cancer cells and preventing and treating senile dementia.
US20080089931 EphA2, EphA4 and LMW-PTP and methods of treatment of hyperproliferative cell disorders The present invention relates to methods and compositions designed for treatment, management, or prevention of a hyperproliferative cell disease, particular cancer. The methods of the invention comprise the administration of an effective amount of a composition that targets cells expressing low molecular weight protein tyrosine kinase (“LMW-PTP”) in particular using moieties that bind an Eph family receptor tyrosine kinase, such as EphA2 or EphA4, and inhibits or reduces LMW-PTP expression and/or activity. In one embodiment, the method of the invention comprises administering to a subject a composition comprising an EphA2 or EphA4 targeting moiety attached to a delivery vehicle, and one or more agents that inhibit LMW-PTP expression and/or activity operatively associated with the delivery vehicle. In another embodiment, the method of the invention comprises administering to a subject a composition comprising a nucleic acid comprising a nucleotide sequence encoding an EphA2 or EphA4 targeting moiety and an agent that inhibits or reduces LMW-PTP expression and/or activity. In yet another embodiment, the method of the invention comprises administering to a subject a composition comprising an EphA2 or EphA4 targeting moiety and a nucleic acid comprising a nucleotide sequence encoding an agent that inhibits or reduces LMW-PTP expression and/or activity, where the nucleic acid is operatively associated with the delivery vehicle. Pharmaceutical compositions are also provided by the present invention.
WO2007084221A3 Methods and apparatus for identifying subject matter in view data The present invention relates to the compound AMG 706, of formula I, and in particular to solid-state forms of that drug to pharmaceutical compositions comprising such solid-state forms, and to processes for preparing them. i
CN1965939A Externally applied formulation for treating skin amyloidosis The invention relates to an external agent for treating amyloidosis of skin, wherein its active components comprise 70-150g pokeberry, 100-200g black plum, 300-400g gallnut, 200-300g dittany bark, 70-140g centella, and 1-3g camphor. And the production comprises that: putting into boiling container, adding 4000-5000ml distilled water, boiling for more than 10h with warm fire; filtering out slag; evaporating, and breaking the left solid into powder, mixing 50g powder, 10g trolamine, 10g ethal, 100g Vaseline, 93g stearic acid, 93g monostearate, 1g methyl-p-hydroxybenzoate ethyl, 40g glycerin, and 440ml distilled water, into external agent which uses oil to pack water. The inventive agent has no toxicity and no side effect.
US20110236441 Antimicrobial substrates and uses thereof A new substrate makes it possible to modify surface properties relating to antimicrobial properties. Said substrate has an electron donating surface, characterized in having metal particles on said surface, said metal particles comprising palladium and at least one metal chosen from gold, ruthenium, rhodium, osmium, iridium, and platinum, wherein the amount of said metal particles is from about 0.001 to about 8 μg/cm2. The substrate is suggested for different uses, such as for modifying the hydrophobicity, protein adsorption, adhesion of bacteria, as well as preventing bacterial transmission and in particular preventing nosocomial infections.
CN101822832B Composition with anti-tumor effect and application thereof in preparing medicament for treating tumor The invention provides a composition with anti-tumor effect and application thereof. The composition consists of 0.01 to 10 weight parts of pure bufadienolide compound, extract rich in bufadienolide compound, raw toad venom or toad skin and 0.01 to 99.9 weight parts of medicament with anti-arrhythmic effect. The composition with the anti-tumor effect has the advantage that the match among the components is scientific and reasonable; multiple in vitro tumor cytotoxicity and in vivo tumor inhibiting experiments show that the composition provided by the invention has good anti-tumor effect and plays a role in synergy after combination; and cardiotoxic experiments show that the cardiotoxicity of the composition provided by the invention is obviously reduced, and the composition can reduce thecardiotoxicity caused by primary single use of the bufadienolide compound, the toad venom or the toad skin and plays a role in detoxifying. Therefore, the composition is safer and more effective to use, and is expected to develop a new generation anti-cancer medicament.
DE102006021572A1 Use of taurolidine for preparing a medicament for preventing/treating e.g. immunodeficiency and autoimmune disorder Use of taurolidine (I) for preparing a medicament for preventing/treating immunodeficiency. - ACTIVITY : Immunosuppressive; Antimicrobial; Antiarthritic; Antirheumatic; Anti-HIV; Antiinflammatory; Dermatological; Cytostatic. - MECHANISM OF ACTION : None given.
CN101485687B Medicament for treating gastrointestinal tract disease using biological viable bacteria The invention discloses a medicine for treating gastrointestinal diseases by utilizing biological live bacteria, which is prepared from the following substances: 1 to 6 weight portions of oligoisomaltose, 1 to 6 weight portions of glucose, as well as 1 to 10 hundred million CFU/gram of bifidobacteria, 1 to 10 hundred million CFU/gram of lactobacilli and 1 to 10 hundred million CFU/gram of probiotics which take the total weight of the oligoisomaltose and the glucose as a radix number, wherein the probiotics are at least one of bacillus, lactococcus and enterococcus. The medicine is based on a modern microecology theory, adopts a probiotic live bacteria preparation to treat diseases such as gastritis, gastric ulcer, enteritis, diarrhea, constipation, indigestion, abdominal distension, diarrhea, intestinal cancer, acute and chronic hepatitis, low immunity and the like, and has the advantages of reliable action, broad function, safe use, no any toxic side effect and irritation, convenient administration and carrying and the like.
CN102614193A Use of progesterone in preparation of drug for treating and recovering infant encephalopathy The invention relates to a use of progesterone in preparation of a drug for treating and recovering infant encephalopathy. The drug containing progesterone can be processed into an intravenous injection, a muscle injection or a subdermal implant by different methods and is used for treating anomaly encephalopathy such as hypoxic-ischemic brain damages, cerebral palsy and epilepsia caused by infant birth injuries or extruded cerebral trauma. The use of progesterone in preparation of a drug for treating and recovering infant encephalopathy is a novel use. The invention also provides the dosage forms, administration methods and dosages of the drug containing progesterone. Progesterone is safe and non-toxic, has obvious pharmacological effects, greatly reduces a mortality rate of babies having birth injuries, and reduces and even prevents cerebral palsy and disability caused by injuries. Therefore, the progesterone has a great clinical application meaning.
CN1796381A Compound for treating B type hepatitis and medication composition This invention provides a compound for hepatitis B therapy, with a structural formula I or II. This invention also relates to a blended composite drug for hepatitis B therapy which contains effective dose of the compound mentioned above in. Besides, this invention still provides a drug combination for hepatitis B therapy which includes effective dose of the compound mentioned above and pharmacologically acceptable adjuvant drugs, carriers or vehicles.
US20120321716 Technology for preventing abuse of solid dosage forms Abuse resistant pharmaceutical formulations are provided that contain one or more abusable drugs and one or more abuse deterrent components. The abuse deterrent component(s) prevent the abusable drug(s) from being removed/extracted to an appreciable extent and/or rate. The abuse deterrent component(s) may be in the form of pellets, beads, beadlets, granules, powders, or the like, and may comprise a core that contains a material that is both hydrophilic and hydrophobic, and optionally a pH-dependent coating.
US20090170798 Highly safe intranasally administrable gene vaccines for treating alzheimer's disease An objective of the present invention is to provide a safe and effective vaccine therapy for Alzheimer's disease. A minus strand RNA viral vector carrying amyloid gene was constructed, and administered intranasally to 24- to 25-months-old APP transgenic mice. The level of serum anti-A 42 antibody was determined and showed to be markedly higher than the control. The results of histological investigation showed that the administration of a vector of the present invention markedly reduced senile plaques in all of the frontal lobe, parietal lobe, and hippocampus. The brain A level was also markedly reduced. Furthermore, the administration of a vector of the present invention did not result in lymphocyte infiltration in the central nervous system.
WO2013049722A1 Compounds useful as inhibitors of atr kinase The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; solid forms of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I-l : wherein the variables are as defined herein. Additionally, the compounds of this invention have formula II: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein.
CN101759754A Synthetic method of beta-Sitosterol Nicotinate The present invention discloses a synthetic method of Beta-Sitosterol Nicotinate. Under a dry condition without water, the Beta-Sitosterol Nicotinate is synthesized in organic solvent by using Nicotinoyl chloride and Beta-Sitosterol. The optimum technological condition is ensured that n (Beta-Sitosterol): n (Nicotinoyl chloride): n (pyridine) is 1:4:12; the reaction temperature is 91 DEG C, and the reaction time is 6 hours; pyridine is used as solvent and disacidify, and 95% of ethanol is used for recrystallization. The yield can reach more than 75%. The present invention has the advantages of few steps, simple operation, high yield, and is suitable for industrial production.
US20080188544 Lyophilized formulations of salinosporamide a Lyophilized formulations comprising Salinosporamide A or analogs thereof are provided. In some aspects, lyophilized formulations comprising Salinosporamide A or analogs thereof and bulking agents are provided. Also provided are methods of lyophilizing Salinosporamide A or analogs thereof. In some aspects, a solvent or co-solvent system is utilized. Also provided are methods of administering Salinosporamide A or analogs thereof to patients.
US20110257159 Orally disintegrating tablet formulations of mirtazapine and process for preparing the same Silicon dioxide free orally disintegrating tablet formulations of mirtazapine or a pharmaceutically acceptable salt thereof having crospovidone and sodium stearyl fumarate and one or more pharmaceutically acceptable excipients and a process for preparing such a formulation.
US20080070986 surfactants esters of citric acid with ethoxylated fatty alcohols for applying to skin, preventing pathogenic bacteria like Propionibacterium, Staphylococcus; without impairing the natural balancing processes, maintain natural pH value (acid protection jacket of the skin) The invention relates to the use of alkylether citrates in cosmetic and pharmaceutical preparations for protecting and maintaining the natural skin/mucous membrane microflora and the microbial skin/mucous membrane ecosystem without impairing the natural balancing processes which limit the number of pathogenic bacteria so that they do not become disease-inducing.
CN1899295B Use of kakonein in preparing medicine for treating endometriosis The present invention discloses the application of puerasin in preparing medicine for treating endometriosis. Animal test proves the obvious endometriosis treating effect of puerasin, and what is more important is that puerasin possesses inapproachable safety compared with danazol. With high treating effect and basically no adverse effect, puerasin possesses excellent application foreground in treating endometriosis.
US20100137403 Method for enhancing cognition or inhibiting cognitive decline A method for enhancing cognition or inhibiting cognitive decline in a subject comprises selecting a Ca2+ channel blocker that is effective, when administered intravenously to an animal in a nontoxic amount, to increase NF-κB expression in the brain of the animal; and administering the selected Ca2+ channel blocker to the subject, via a systemic route that affords an adequate therapeutic window for cognition-enhancing or cognitive decline-inhibiting effectiveness of the selected Ca2+ channel blocker, in an amount within the therapeutic window. The selected Ca2+ channel blocker can be, for example, tiapamil or a pharmaceutically acceptable salt or prodrug thereof.
EP2528920A2 Bicyclic heteroaryl derivatives having inhibitory activity for protein kinase The present invention relates to a novel bicyclic heteroaryl derivative, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a solvate thereof having an improved inhibitory activity for protein kinases, and a pharmaceutical composition for preventing or treating an abnormal cell growth disorder comprising same as an active ingredient.
CN102805743A Application of arctigenin in treating angiogenesis diseases The invention provides a novel medical application of arctigenin, belonging to the field of medicine. According to the application of arctigenin in treating angiogenesis diseases provided by the invention, the arctigenin is applied to treating angiogenesis diseases, a good angiogenesis inhibiting effect is shown in a chorioallantoic membrane model test of a chicken embryo, which reminds that the arctigenin can be applied to treatment or auxiliary treatment of angiogenetic diseases. The medical application of arctigenin which inhibits angiogenesis reminds that the arctigenin has wide medical application prospect in treating diseases such as tumor and other pathological angiogenesis diseases such as diabetic retinopathy, psoriasis, atherosclerosis, rheumatoid arthritis and the like.
US7034020 inactivators of antigen-specific T cells; increased half-life The present invention provides a series of compounds having structural formulas wherein n1 is 1 to 5, n2 is 1 to 4 and m is 1 to 3; X is O or NH; Y is CH2, O, S, NH, NR; R is selected from the group consisting a straight-chain aliphatic group, a branched-chain aliphatic group and an alicyclic group; wherein R′ is selected from the group consisting of hydrogen, methyl and ethyl; when Y is O, n1 is not 1; and wherein X and R′ are independently optionally substituted at C2, C3 or C4 in compounds of Fomula IV or a pharmaceutically acceptable salt thereof. Also provided is a method of inactivating antigen-specific T cells in a n individual.
US20100080847 Medicinal compositions quickly disintegrating in the oral cavity and process for producing the same This invention relates to a medicinal composition, which rapidly disintegrates when taken in the oral cavity and shows sufficient hardness upon production, distribution and use in usual manner, can be obtained by adding, to a sugar alcohol and/or saccharide, a sugar alcohol and/or saccharide having a lower melting point than the first-mentioned sugar alcohol and/or saccharide and then subjecting the resulting powder to combined processing of compression and heating. This invention can provide medicinal compositions, which rapidly disintegrate when taken in the oral cavity without water and are excellent in handling ease owing to exhibition of sufficient hardness upon their production, transportation and use in usual manner, and can also provide a process for the production of the medicinal compositions, which is simpler and can avoid contact between an active ingredient and water as needed.
DE102006010643A1 Using quaternary ammonium compounds to inhibit precipitation of fluoroquinolone antibiotics, particularly in ready-for-use formulations for veterinary medicine Use of quaternary ammonium compounds (A) for inhibiting precipitation of fluoroquinolones (FQ) from their solutions. An independent claim is included for a pharmaceutical composition that contains (A) and (FQ) in dissolved form. - ACTIVITY : Antibacterial. No details of tests for antibacterial activity are given. - MECHANISM OF ACTION : None given.
US20120149699 IMIDAZO[1,2-a]PYRIDINE SULFONAMIDES AS TRPM8 MODULATORS Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, and are defined herein.
US7662845 2,5-Dioxoimidazolidin-4-yl acetamides and analogues as inhibitors of metalloproteinase MMP12 The invention provides compounds of formula in which L, X, Y, Z1, Z2, R1, R2, R3 and G2 have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
CN101601750A Specific beriberi medicament The invention provides a specific beriberi medicament, which is mainly prepared from the following raw materials in portion by weight: 3 to 12 portions of calcined alum, 1 to 4 portions of almond, 0.25 to 1 portion of metronidazole tablet, 0.15 to 1 portion of nystatin tablet, 0.15 to 1 portion of furazolidone tablet, 0.25 to 1 portion of oxytetracycline tablet, 0.15 to 1 portion of vitamin B1 tablet, 0.25 to 1 portion of vitamin B2 tablet, and 10 to 30 portions of clotrimazole cream. The medicament takes antibacterial medicaments as main ingredients, and can kill bacteria and fungi which cause the beriberi; the adding of vitamin B complex and vitamin C aims to repair wound surfaces, promote the healing, and ensure that the skin restores to normal more quickly; the calcined alum ensures that medicament application positions keep relatively dry; the almond relieves internal heat; various components supplement each other, can quickly and effectively treat the beriberi, and enables patients to recover; and at the same time, the medicament also has better efficacies in treating sole sweating and foot odor.
CN101972255A Rosiglitazone hydrochloride-containing pharmaceutical composition and preparation method thereof The invention relates to a rosiglitazone hydrochloride-containing pharmaceutical composition, which is characterized in that: the composition consists of rosiglitazone hydrochloride, lactose, starch, low-substituted hyprolose, adhesive and magnesium stearate, with the proportions (in part by weight) as below: 0.5 to 5 parts of rosiglitazone hydrochloride, 10 to 90 parts of lactose, 20 to 80 parts of starch, 2 to 8 parts of low-substituted hyprolose, 10 to 90 parts of adhesive and 0.2 to 5 parts of magnesium stearate. In the preparation method according to the invention, high-substituted hyprolose takes the place of polyvidone and is used as the adhesive, which not only settles the problems of the shift of characteristic peak and failing to detect principal medicine, but also dramatically improves the flowability and tablettability of the resultant granules without an prominent impact on other indexes of product.
WO2010062221A1 Substituted 2-(5-hydroxy-2-methyl-1n-indole-3-il) acetic acids and ethers thereof and the use of same to treat viral diseases The invention relates to new substituted 2-(5-hydroxy-2-methyl-1n-indole-3-il) acetic acids, new antiviral active agents, pharmaceutical compositions, antiviral medicinal agents and a method for preventing and treating viral diseases, in particular diseases caused by the influenza virus and the infectious hepatitis C virus (HCV). New substituted 2-(5-hydroxy-2-methyl-1n-indole-3-il) acetic acids and ethers thereof of the general formula 1 as well as pharmaceutically acceptable salts and/or hydrates thereof are proposed, where R1 is an amino group substituent selected from a hydrogen atom, an optionally substituted C1-C5 alkyl, acyl or sulphonyl; R2 and R4 independently from each other represent an alkyl substituent selected from a hydrogen atom, a halogen atom, an optionally substituted C1-C3 alkyl, optionally substituted hydroxyl, an optionally substituted amino group, optionally substituted amino methyl and a substituted mercapto group; R3 is hydrogen and optionally substituted lower alkyl C1-C5; R5 is a cyclic system substituent selected from a hydrogen atom, fluorine atom, trifluormethyl, carboxyl, alkyloxycarbonyl, possibly substituted aryl, heterocyclyl, optionally substituted amino methyl and a cyano group; R6 represents a hydroxyl substituent selected form a hydrogen atom, optionally substituted lower alkyl C1-C5 and acyl.
WO2009006413A1 Substituted pyrrolidines Disclosed herein are substituted pyrrolidine-based muscarinic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof. Formula (I):
WO2013166621A1 1-(dihydronaphthalenyl)pyridones as melanin-concentrating hormone receptor 1 antagonists This invention relates to novel 1-(dihydronaphthalenyl)pyridones which are antagonists of the melanin-concentrating hormone receptor 1 (MCHR1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of obesity and diabetes.
WO2008014219A3 Thiozolidinedione derivatives as p13 kinase inhibitors Invented is a method of inhibiting the activity/function of PB kinases using thiozolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiozolidinedione derivatives.
WO2010083501A3 Alpha-helix mimetic using a 2,5-oligopyrimidine scaffold Alpha-helix mimetics and associated methods of making are provided. These compounds are constructed using a 2,5-oligopyrimidine scaffold. The semi-rigid scaffold holds individual side chain-like residues in orientations that mimic the orientations of side chain residues of an ?-helical protein domain. The new scaffold is easier to make than previous scaffolds and has much more favorable physical properties than previous alpha-helix mimics. The amphiphilic alpha-helix mimetics have application for making libraries and for treating diseases or conditions effected by the inhibition or disruption of interactions with the alpha helix of a protein.
CN102274210A Applications of ineupatorolide B in preparation of antitumor drugs The invention discloses a medicinal purpose of ineupatorolide B. The medicinal purpose of ineupatorolide B comprises applications of ineupatorolide B in preparation of antitumor drugs, drugs for treating cervix tumors of human bodies, and drugs for inhibiting cell proliferation of lung tumors of small cells of human bodies. The inventors of the invention invent the applications of ineupatorolide B in the preparation of the antitumor drugs because the inventors find new pharmacological activities of ineupatorolide B by researching for a long term. According to the invention, a new choice is provided for people to prepare anticancer drugs.
EP2528902A1 Oxygen-substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
US20110021482 Novel N-Benzylamide Substituted Derivatives of 2-(Acylamido)acetic Acid and 2-(Acylamido)propionic Acids: Potent Neurological Agents A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula I or Ia: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
CN103432119A Matrix formula and preparation method of fat-soluble indometacin salbutamol suppository The invention provides a matrix formula and a preparation method of a fat-soluble indometacin salbutamol suppository. The suppository comprises indometacin, salbutamol sulfate and polyoxyethylene stearate. The suppository overcomes the defects of embrittlement, layering, inhomogeneity and the like, and is smooth to produce and stable in quality.
US20050101641 Aromatic sulfone hydroxamic acids and their use as protease inhibitors This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
US20110237543 Composition for Prevention or Treatment of Eye Diseases Provided is a composition for prophylaxis or treatment of an eye disease comprising a compound represented by General Formula I: S-(MS)p-(MS)q General Formula I wherein S represents sialic acid, and (MS)p and (MS)q independently represent a monosaccharide residue. The compound used as the active ingredient inhibits expression of MMP-9 and inflammation-mediated cytokines (IL-1β, TNF-α, etc.) in corneal epithelial cells and inhibits VEGF-mediated VEGFR-2 activation in human retinal endothelial cells (HREC), thereby exhibiting prophylactic or therapeutic activity for eye diseases such as dry eye syndrome, inflammatory eye disease, neovascularization-associated eye disease and side effects of wearing of contact lenses. Also, because it has no cytotoxicity or skin side effect, the provided composition may be safely used as a pharmaceutical composition, a neutraceutical composition or a food composition. In addition, the composition may be used as a cleaner or a lubricant for contact lenses since it has nonbacterial antiinflammatory activity and ocular contact lubricating activity.
WO2011054922A1 Salts of fused pyrazine compounds, useful for the treatment of degenerative and inflammatory diseases. Novel salts of a [1.2.4]triazolo[1,5-a]pyrazine compound according to Formula (I): the salts may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammation, and others. The compounds are inhibitors of MAPKAPK5 activity and are useful for the treatment of diseases involving the abnormally high expression of MMP activity.
CN102250094A 2-alkylthio-9-alcoxyalkyl adenine compound and synthesis thereof The invention discloses a 2-alkylthio-9-alcoxyalkyl adenine compound and synthesis thereof. The chemical structural formula of the compound is shown in the specifications. The synthesis method comprises the following steps of: (a) reacting 2-mercaptoadenine I with alkyl halide X-R1 under the alkaline condition to obtain 2-alkylthio adenine II; and (b) synthesizing the 2-alkylthio-9-alcoxyalkyl adenine compound III by the 2-alkylthio adenine II and p-toluenesulfonate TsO(CH2)2OR2. The method has the advantages of short reaction time, a few reaction steps and high yield; ideal experimental results can be obtained; and the synthesized compound has potential platelet aggregation inhibiting activity.
CN102670939A Compound propolis composition for treating livestock acariasis and preparation method thereof The invention relates to a compound propolis composition for treating livestock acariasis and a preparation method thereof. The composition is prepared by mixing the following components in parts by weight: 15-35 parts of propolis, 15-35 parts of straight ladybell root, 15-35 parts of common anemarrhena, 15-40 parts of large-leaved gentian, 15-45 parts of gypsum, 15-35 parts of rhubarb, 15-35 parts of great burdock achene, 15-35 parts of weeping forsythia, 15-35 parts of baikal skullcap root, 15-35 parts of fructus gardenia, 15-55 parts of dried orange peel and 15-35 parts of skunk bugbane. The compound propolis composition has the beneficial effects of reasonable composition, easiness for preparing, freeness from toxic and side effects, environment friendliness, no medicament residues, no medicament tolerance, ultrafine grinding, high bioavailability, and very remarkable curative effect; and as proved by clinic, the compound propolis composition has a special treatment effect on livestock acariasis.
CN103720679A Application of Shikonin in medicine for treating acute leukemia The invention relates to an application of a natural compound, and relates to a new application of Shikonin, and an application of Shikonin in preparation of medicines for treating acute leukemia. The English name of the Shikonin is Shikonin, the CAS No. is 517-89-5, a molecular formula is C16H16O5, the molecular weight is 288.3, and a chemical name of the Shikonin is 5,8-dihydroxy-2-(1-hydroxy-4-methyl-3-penten-1-yl)naphthalene-1,4-dione. The employed Shikonin is extracted from plants or chemically synthesized according to the prior art, the prepared medicines are individual Shikonin or contain other antitumor drug, and an excipient or a carrier of the medicinal preparation. According to the invention, the effectively increased cell active oxygen and an appropriately activated Nrf2 approach to cause the differentiation of acute leukemia cells, so that the form and function of normal cells can be approached or completely possessed. In the provided concentration range, the Shikonin induces the abnormal leukemia cells to be obviously differentiated, and simultaneously appears nonlethal low toxicity effect, so that the Shikonin has good application prospect for preparing the medicines for anti-acute leukemia.
CN102885831A Application of Gypensapogenin A in medicine for treating hemorrhagic fever with renal syndrome The invention discloses a new application of Gypensapogenin A in preparation for a medicine for treating hemorrhagic fever with renal syndrome. Experimental studies on the in-vitro inhibition and the in-vivo inhibition of Gypensapogenin A for hemorrhagic fever with renal syndrome show that Gypensapogenin A has a low toxic effect on cells, plays a role of directly killing the virus of hemorrhagic fever with renal syndrome, can obviously inhibit the multiplication of the virus, and plays an obvious role of protecting hamsters infected with the virus so as to delay the onset time, prolong the disease course and decrease the mortality. Thus, Gypensapogenin A is an effective and safe medicine for treating the hemorrhagic fever with the renal syndrome.
US20090155180 Methods and targets for identifying compounds for regulating rhinovirus infection The present invention provides methods for identifying genes, expression regulators, receptors, protein product receptors, and proteins that may regulate rhinovirus infections. The genes identified may be used as markers for disease onset and progression and to measure efficacy of a therapeutic. The present invention also provides methods to screen agents that are capable of regulating rhinovirus infection. The present invention also provides methods of identifying therapeutic compounds that may treat various disorders by regulating the expression and activity of genes, expression regulators, receptors, protein product receptors, and proteins identified.
US20090181968 Novel 3-Bicyclocarbonylaminopyridine-2-Carboxamides or 3-Bicyclocarbonylaminopyrazine-2-Carboxamides The present invention relates to compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] as well as pharmaceutically acceptable salts and pharmaceutical compositions including the compounds are prepared or thereof: wherein, A1, A2, R1, R2, R3, R4, and R5 and n are as defined in the specification. The compounds of formula (I) are useful in therapy.
US20130045243 NANOGENOMICS FOR MEDICINE: siRNA ENGINEERING Described herein are materials and methods for the delivery of siRNA and the production of nanoparticles useful for the delivery of siRNA. Methods of treating a disease or disorder using the nanoparticles described herein also are disclosed.
CA2679809A1 Benzimidazole derivatives and methods of use thereof The present invention relates to compounds of formula (I); compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IGT) in a patient.
CN103214422A Preparation methods and anti-cancer effect of novel substituted amido imidazolone derivatives The invention relates to the technical field of medicines and specifically relates to preparation methods and anti-cancer effect of novel substituted amido imidazolone derivatives. The structural general formula of the compounds are FORMULA, wherein in imidazolone ring, in the group in the general formula I, R1 or R2 is independently selected from H, C1-C12 saturated or unsaturated alkyls, cycloalkyls or alkenyls, C1-C12 saturated or unsaturated alkyls, cycloalkyls or alkenyls having heteroatoms such as O, N and S, phenyl, benzyl and substituted phenyl on one hand; on the other hand, in the general formula II, group can be a saturated or unsaturated ring group, wherein R3 can be independently selected from H, C1-C12 saturated or unsaturated alkyls, cycloalkyls or alkenyls, C1-C12 saturated or unsaturated alkyls, cycloalkyls or alkenyls having heteroatoms such as O, N and S, and substituted phenyl; X can be selected from O, S, NH, substituted N atom and the like. The compounds are stable in chemical properties and capable of inhibiting growth of tumor cells, and can be used for preparing anti-cancer drugs.
DE102004060998A1 New 2,4-dicyclopentyl-3-(fluoro-(4-trifluoromethyl-phenyl)-methyl)-7, 7-dimethyl-5,6,7,8-tetrahydro-quinolin-5-ol compound is cholesterol ester transfer protein inhibitor useful to treat and/or prevent e.g. coronary heart diseases 2,4-Dicyclopentyl-3-[fluoro-(4-trifluoromethyl-phenyl)-methyl]-7,7-di methyl-5,6,7,8-tetrahydro-quinolin-5-ol compound (I) and its salts and solvate are new. 2,4-Dicyclopentyl-3-[fluoro-(4-trifluoromethyl-phenyl)-methyl]-7,7-di methyl-5,6,7,8-tetrahydro-quinolin-5-ol compound of formula (I) and its salts and solvates are new. Independent claims are also included for: (1) a medicine (A) comprising (I) in combination with an inert and non-toxic auxiliary material; and (2) the preparation of (I). [Image] - ACTIVITY : Cardiant; Antilipemic; Antidiabetic; Antiarteriosclerotic; Vasotropic; Anorectic; Cerebroprotective; Neuroprotective; Nootropic. - MECHANISM OF ACTION : Cholesterol ester transfer protein inhibitor. The ability of (I) to inhibit cholesterol ester transfer protein was tested using biological assays. The results showed that (I) exhibited a median inhibitory concentration value of 55 nM.
CA2730540A1 Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis The invention relates generally to methods for inhibiting angiogenesis. More particularly, methods for inhibiting angiogenesis comprise selectively inhibiting phosphoinositide 3-kinase delta (P13K.delta.) activity in endothelial cells. The methods may comprise administration of one or more cytotoxic therapies including but not limited to radiation, chemotherapeutic agents, photodynamic therapies, radiofrequency ablation, anti-angiogenic agents, and combinations thereof.
US20050119458 Transport protein for use in identifying modulator for prevention and treatment of cell proliferative, skin and psychological disorders; anticonvulsants; insecticides; pesticides; anthelmintics The present invention provides a novel human proton-gated ion channel (hASIC1B) and polynucleotides which identify and encode hASIC1B. The invention also provides genetically engineered expression vectors and host cells comprising the nucleic acid sequences encoding hASIC1B and a method for producing hASIC1B. The invention also provides for use of hASIC1B, and agonists, antibodies or antagonists specifically binding hASIC1B, in the prevention and treatment of diseases associated with expression of hASIC1B. Additionally, the invention provides for the use of antisense molecules to polynucleotides encoding of hASIC1B for the treatment of diseases associated with the expression of hASIC1B. The invention also provides diagnostic assays, which utilize the polynucleotides, or fragments or the complements thereof, and antibodies specifically binding hASIC1B.
WO2007065948A1 Novel n-sulfamoyl-piperidineamides for the prophylaxis or treatment of obesity and related conditions The present invention relates to novel N-sulfamoyl-piperidineamides of general formula (I) and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment of obesity and its concomitant and/or secondary diseases and/or related conditions.
WO2009135000A2 Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-117199 and analogs Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. NSC-117199 was identified as a porent inhibitor of the protein tyrosine phosphatase (PTPa) Shp2. A focused library of analogs incorporating an isatin scaffold was designed and evaluated for inhibition of Shp2 and Shp1 PTP activities. Several compounds were identified that selectively inhibit Shp2 over Shp1 and PTP1B with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.
EP1021148B1 Composition and method for acceleration of wound and burn healing A method for treating wounds including contacting a wound with an effective wound healing amount of bioactive glass and topical antibiotic and composition for the accelerated healing of wounds and burns including particulates of bioactive glass and at least one topical antibiotic.
EP0932600B1 Sulfonamide substituted aspartic acid interleukin-1beta converting enzyme inhibitors The present invention relates to compounds that are inhibitors of interleukin-1β converting enzyme that have Formula (I, II or III). This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, and shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1β converting enzyme.
CN103446103A Applications of Sarcaboside B in medicament against respiratory syncytial virus The invention discloses applications of Sarcaboside B in preparing a medicament against respiratory syncytial virus. Experiments prove that the Sarcaboside B plays a remarkable role in inhibiting respiratory syncytial virus RSV. The applications disclosed by the invention provide an experimental basis for the Sarcaboside B in clinically treating RSV-infected diseases, and offer certain guiding significance for developing medicaments against RSV, thus having an important reference value.
WO2012146169A1 Chinese herbal extract, preparing method and application thereof A Chinese herbal composition with anti-aging effect is characterized in that it comprises the water and/or solvent extracts of the following raw materials in weight parts: 30 to 70 parts of Rhizoma Polygonati, 30 to 70 parts of Rhizoma Polygonati Odorati, 0.01 to 5 parts of gold foil. The said solvent is selected from methanol, ethanol, isopropyl alcohol, n-butanol, ethylene glycol, 1,2-propylene glycol, 1,3-propylene glycol, 1,3-butylene glycol, acetone, ethyl acetate, or the combination thereof. The extract of Chinese herbal the and the Chinese herbal composition comprising it possess the effects of moisturizing skin, repairing, caring and rebirthing, without stimulus to skin. They are used in skin anti-aging, or in cosmetics as active additives, and its cost is lower.
CN101020659A 9-aminoalkylamido-1-azabenznthrone derivative and its synthesis and application The present invention is one kind of 9-aminoalkylamido-1-azabenzanthrone derivative and its synthesis process and application as acetylcholinesterase inhibitor. Experiment shows that 9-aminoalkylamido-1-azabenzanthrone derivative of the present invention has powerful acetylcholinesterase inhibiting performance and excellent inhibiting selectivity, and its inhibiting capacity on acetylcholinesterase is over 1000 times higher than that on butyrylcholinesterase. It is shown that the said compound may be developed into medicine for treating Alzheimer disease, cerebrovascular dementia and similar diseases.
CN102133323A Herbal anesthetic and preparation method thereof The invention discloses a herbal anesthetic which is prepared from the following raw materials in parts by weight: 13-15 parts of venenum bufonis, 8-13 parts of raw szechuan aconite, 7-13 parts of raw wild aconite, 20-25 parts of pepper, 16-20 parts of asarum, 15-18 parts of radix zanthoxyli, 7-10 parts of borneol, 20-30 parts of murraya jasminorage, 4-6 parts of houttuynia, 2-4 parts of gallnut, 6-8 parts of Chinese mugwort leaf, 4-6 parts of bistorta, 4-6 parts of dandelion, 4-6 parts of brucea javanica, 100-130 parts of notoginseng and 600-700 parts of alcohol the concentration of which is 75%. The herbal anesthetic disclosed by the invention is convenient to use and simple to operate, has the advantages of good anesthetic effect, no side effects, safety, reliability and the like, eliminates the pain of patients in the processes of extracting and treating teeth, eliminates the fear of patients, is popular among patients, especially enables the deciduous teeth of children to be replaced painlessly, conveniently and quickly, lowers the allergic probability, reduces the postoperative hemorrhage, and prevents the infection.
CN101880222A Square acid derivate and preparation method thereof The invention provides square acid derivate and pharmaceutical salt thereof. The square acid derivate has a structure shown as the formula (I). The square acid derivate can be taken as micro-molecular tubulin inhibitor, having the function of resisting microtubule and remarkable anti-tumor activity and the advantages of small molecular weight, simple synthesis and small toxic and side effects. The invention further provides a synthesis method of the square acid derivate and an anti-tumor medical composite taking the square acid derivate and the pharmaceutical salt thereof as active components.
CN102920665A Colon-targeted zinc oxide pellet and preparation method thereof The invention discloses a colon-targeted zinc oxide pellet, solving the problems of high additive amount, multiple side effects and poor release effect of zinc oxide products in the prior art. The colon-targeted zinc oxide pellet comprises a pellet core consisting of 50-60% by weight of zinc oxide and 30-40% by weight of an auxiliary material and 10-20% by weight of a colon-targeted coat dissolved in a colon-targeted section rather than the stomach. The invention further provides a preparation method of the colon-targeted zinc oxide pellet. The pellet disclosed by the invention can be ensured to be dissolved in the colon-targeted section rather than the stomach so that targeted locating treatment effect of the colonic disease can be taken and the treatment effect of diseases is improved; and meanwhile, the pellet is available in raw materials, rational in formula, low in production cost, simple in technological process and easy to popularize and use.
CN103239707A Eye drop for treating myopia The invention discloses an eye drop for treating myopia. The eye drop comprises the following components in parts by weight: 4-7 parts of flos chrysanthemi indici, 3.5-3.9 parts of honeysuckle, 9-10 parts of cuscuta chinensis, 3-3.9 parts of oleum menthae, 6-9.8 parts of silver ion solution, and 4-8.9 parts of mulberry silk fiber. The eye drop can alleviate asthenopia.
WO2013088389A1 Linezolid premix The present invention relates Linezolid premix and process for the preparation of the said premix. The present invention also relates to pharmaceutical compositions comprising said Linezolid premix.
WO2009080693A3 Pharmaceutical composition comprising tesofensine or its analogue and a beta blocker This invention relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a compound of Formula I and a beta blocker. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating obesity or an obesity associated disease.
CN101161652B Quinolizine derivatives having antibacterial activity The present invention relates to novel quinolizidine derivatives with antibiotic activity, the preparation method thereof, and medicine combination containing the compounds, as well as the application of the compounds to the fields of treatment/prevention on contagious diseases. The present invention belongs to the medicine technology field. Based on research, the quinolizidine derivatives with antibiotic activity provided by the present invention has the advantages of antibiotic effect with extended spectrum, high efficiency and low risk of drug tolerance, thereby being excellent in clinicalapplicable value, and capable of being used widely in clinic.
WO2011053705A1 Pyrimidine compounds as delta opioid receptor modulators Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, and L, A, and Ra are defined herein.
US20120121679 Viricidal and microbicidal compositions and uses thereof The present disclosure encompasses compositions comprising a surfactant, and an acid such as, but not limited to, levulinic acid, that together have a synergistic effect in reducing the viability of a virus population compared to the efficacy of the individual compounds. This synergy allows the formulation of compositions where the active agents (including an acid and a surfactant) are present at concentrations effective to inactivate viruses on surfaces, including human skin. The viricidal compositions disclosed herein are efficacious without damaging the surface to which they may be applied, or even altering the organoleptic properties of a treated food substance. The viricidal compositions and wipes containing such compositions are suitable for sanitizing any surface suspected of having a viral load thereon, or where it is desirable to ensure that a viral load is as low as possible.
EP1307565B1 Vaccins against marek's disease virus (mdv) and varicella zoster virus (vzv) The invention relates to the field of so-called host cell-associated herpesviruses such as Marek's disease like virus (MDV) of poultry and of Varicella Zoster virus (VZV) of man and to vaccination against disease caused by these viruses. The invention provides a vaccine directed against an infection caused by an herpesvirus that is essentially host cell associated comprising a recombinant viral genome derived from said herpesvirus, said genome allowing recombination essentially free of said host cell.
CA2136492C Pharmaceutical composition containing diclofenac and 2-hydroxypropyl-.beta.-cyclodextrin A method of preparing an injectable pharmaceutical or veterinary composition which comprises either diclofenac or a salt thereof and 2-hydroxypropyl beta-cyclodextrin, or an inclusion complex of diclofenac or a salt thereof and 2-hydroxypropyl beta-cyclodextrin, includes the step of dissolving either the diclofenac or salt thereof and the 2-hydroxypropyl beta-cyclodextrin, or the inclusion complex, in water to form a solution, the water having been acidified to a pH such that the pH of the solution is from 6,0 to 8,5 inclusive, in the absence of a phosphate buffer. The composition so produced has good stability on storage.
US7015223 Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
CN103251556A Aprepitant nanosuspension and preparation method thereof The invention belongs to the technical field of medicines, and discloses an aprepitant nanosuspension and a preparation method thereof. As aprepitant is small in solubility in water and lower in the oral bioavailability, popularization and use of aprepitant are limited. The aprepitant nanosuspension provided by the invention is characterized by comprising aprepitant, copovidone PVPS630 and povidone PVPK-90 by mass ratio of (4-10):(1-2):(1-2). The preparation method of the aprepitant nanosuspension is mild in condition and simple and controllable, and higher oral bioavailability of aprepitant is realized.
WO2008090140A1 Aryloxypropanolamines, methods of preparation thereof and use of aryloxypropanolamines as medicaments This invention relates to novel aryloxypropanolamines. The invention also relates to the pharmaceutically acceptable salts and solvates containing said compounds, methods for the preparation thereof and to respective synthetic intermediates. Said compounds have agonistic activity at β3 adrenergic receptors and are useful for treatment of ailments influenced by activation of β3 adrenergic receptors.
US6858236 Nutriceutical and drug compositions containing a plant extract or concentrate from the genus Lycopersicon (tomato); bone disorders, e.g., Paget's disease, tumor-induced bone disease or particularly osteoporosis; metabolic disorders The present invention is concerned with nutritional or pharmaceutical compositions containing an extract or concentrate of a plant from the genus Lycopersicon. The compositions of the invention are useful for the treatment or prophylaxis of diseases or conditions which are characterized by increased bone resorption, such as Paget's disease, tumor-induced bone disease or particularly osteoporosis.
US20090017097 Hydrogel polymeric compositions and methods Some aspects of this disclosure relate to a method of treating an opthalmic disease affecting an eye of a patient comprising forming a covalently-crosslinked hydrogel in situ at a peri-ocular, intra-ocular, or intra-vitreal site for controlled release of a therapeutic agent.
US20100240706 1,3-disubstituted-4-phenyl-1h-pyridin-2-ones The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
CN102579319A Slow release composition with cefaclor The invention relates to the technical field of medicine preparation, in particular to slow release composition with cefaclor, which comprises materials by weight: 60% to 90% of the cefaclor, 5% to 20% of hydroxypropyl methylcellulose, 0.5% to 5% of a potential of hydrogen (pH) adjusting agent and 3% to 18% of a porogen. The slow release composition with the cefaclor can be completely released in 4 to 7 hours, thereby being good in release characteristics.
US6894049 Anticancer agents; water solubility The present invention relates to platinum antitumor drugs. In particular, it relates to platinum complexes having formula Ia or Ib or a pharmaceutically acceptable salt thereof wherein: each A is independently an anion; each B is independently halo, hydroxy, carboxylate, carbamate or a carbonate ester, Z is a substituted 5- or 6-membered, heterocyclic moiety wherein at least one substituent sterically hinders access of the Pt atom to a DNA strand of a tumor cell, and wherein Z is other than pyridine; and X is NH3 or mono- or dialkyl substituted NH3. which are active against cancer cells and have improved aqueous solubility and activity.
US20110206620 Therapeutic Compositions for the Treatment of Dry Eye Disease Described herein are materials and methods for treating dry eye disease in a subject.
CA2535527A1 Immunogenic hiv compositions and related methods The invention provides immunogenic compositions which enhance the duration and strength of the immune response in a mammal. The immunogenic compositions contain an HIV antigen, an immunomer and an adjuvant. The HIV antigen can be a whole-killed HIV virus devoid of outer envelope protein gp120. Alternatively, the HIV antigen can be a whole-killed HIV virus, or a p24 antigen. Also provided are kits, the components of which, when combined, produce the immunogenic compositions of the invention. The invention also provides methods of making the immunogenic compositions, by combining an HIV antigen, an immunomer and optionally an adjuvant. The invention further provides a method of immunizing a mammal, by enhancing an immune response in the mammal by administering to the mammal an immunogenic composition containing an HIV antigen, an immunomer and optionally an adjuvant. Also provided is a method of inhibiting in a mammal by administering to the mammal an immunogenic composition containing an HIV antigen, an immunomer and optionally an adjuvant.
CN101732458B Compound essential oil having functions of refreshing spirit, restoring consciousness and resisting fatigue, and wet tissue containing same The invention discloses a compound essential oil having functions of refreshing spirit, restoring consciousness and resisting fatigue, and a wet tissue containing the same. The compound essential oil is prepared by the following raw materials in parts by weight: 20-50 parts of peppermint camphor, 0.5-2 parts of Ylang Ylang flower oil, 15-25 parts of lavender oil, 3-10 parts of rosemary leaf oil, 20-30 parts of sweet orange oil, 15-25 parts of eucalyptol, 20-40 parts of lemon leaf oil, 0.1-0.2 part of peppermint oil, 20-50 parts of clove oil and 30-55 parts of spearmint oil. The invention adopts pure natural plant ingredients, utilizes the characteristics of various aromatic plant active ingredients, such as strong seepage force, high dissolubility and the like, functions in virtue of skins, channels and collaterals, and acupuncture points for seepage and absorption, has obvious curing effect, is suitable for curing various apocamnosis such as eyestrain, brain fatigue, physical fatigue, dizziness, lassitude, sleepiness, strength lacking and the like, has extremely good effect in refreshing spirit, restoring consciousness, relaxing nervus, eliminating dysthesia, stabilizing sentiment and strengthening stamina.
CN1883486A Method for preparing compound double-layered tablet of carisoprodol-aspirin The invention relates to the process for preparing double layer compound tablets of Carisoprodol and Aspilin as skeletal muscle relaxant, which comprises making Aspirin enteric granules, the carrying out pelletization to Carisoprodol through double layered pelleting machines.
US20090105216 3- (aminomethyliden) 2-indolinone derivates and their use as cell proliferation inhibitors The present invention encompasses compounds of general formula (1) wherein R1, R2, R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
EP2167042A2 Pharmaceutical aerosol compositions comprising fluticasone The present invention relates to pharmaceutical compositions and in particular to suspension aerosol pharmaceutical compositions, processes to obtain them and their use in inhalation therapy.
US20120251545 Therapeutic Combinations Of Hydroxybenzamide Derivatives As Inhibitors Of HSP90 The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.
US20110230473 Methods and Compositions for Treating Status Epilepticus and Seizures Causing Status Epilepticus Disclosed herein are methods, kits and compositions for treating, preventing, inhibiting, or reducing a seizure, status epilepticus, neuropathogenesis or a neuropathology caused by overstimulation of the NMDA receptor pathway and/or exposure to an OP compound.
US20060111433 Administering bergapten; modulate the expression of genes for gamma-globin in the human cell line K562; genetic blood disorders The use of angelicin and its structural analogues for the preparation of a medicament for the therapeutic treatment of beta-thalassaemia is described. A structural analogue which is particularly preferred for this purpose is bergapten.
WO2008107910A2 Use of caralluma extracts in the inhibition of adipogenesis and a method of inhibition for the same Inhibition of adipogenesis by the pregnane glycosides(PGs)(or by caralluma extracts) is disclosed. Said inhibition occurs early in the cell cycle which substantially comes to rest at the G1 phase, the action being by the inhibition of the formation of the cyclin D1-CDK 4/6 complex, the prevention of the translocation of said complex into the nucleus and enhancement of the action of cell division inhibitory factors arising during the cell division process in 3T3-L1 cell lines. PG mixtures(including isomer mixtures) exhibit synergy, the preferred mixture being that of the caratubersides and boucerosides in the ratio 9: 1 to 19: 1 w/w. Applications include said inhibition, the treatment/management of obesity and obesity-related disorders, the regulation of obesity-related parameters such as weight, b.p., cholesterol, blood sugar and others and preventing the weight exceeding the critical limit whereat said adipogenesis is triggered in human and animal subjects.
CN102203078A P38 MAPK kinase inhibitor There is provided a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, including all tautomers thereof, compositions comprising the same, use of said compound and compositions for treatment, in particular for the treatment of asthma and COPD, and processes for the preparation of said compound.
EP2305287A1 Combination therapy for eradicating detectable HCV-RNA in antiviral treatment naive patients having chronic hepatitis C infection Use of ribavirin and interferon alpha to prepare pharmaceutical compositions for treating antiviral treatment naive patient having chronic hepatitis C genotype I infection and a viral load of greater than 2 million copies per ml of HCV-RNA as measured by quantitative PCR to eradicate detectable HCV-RNA involving a combination therapy using a therapeutically effective amount of ribavirin and a therapeutically effective amount of interferon-alpha for a total time period of 40 to 50 weeks are disclosed.
US20080249082 Use of Memantine (Namenda) to Treat Autism, Compulsivity and Impulsivity The present invention relates to the treatment of compulsive, impulsive and pervasive developmental disorders. More particularly, the methods described herein comprise administration of memantine to an individual suffering from such a disorder in an amount effective to relieve one or more symptoms of said disorder. In particularly preferred aspects, the invention is directed to the use of memantine for the treatment of autism
CA2355860C Dosage forms comprising porous particles A dosage form comprising a plurality of particles having interior pores and a liquid, active agent formulation in the pores, the particles being compactable and adapted to retain substantially all of the liquid active agent formulation within the pores during the compacting process, is described. The dosage forms may be in the forms of unitary oral forms for immediate release of active agent, prolonged delivery forms, or controlled delivery forms.All forms involve certain absorbent materials having prescribed characteristics, particularly spray dried calcium hydrogen phosphate and magnesium aluminometasilicate.
EP0927163B1 Preparation of 1-butyl-4-piperidinylmethylamine A process for the preparation of 1-butyl-4-piperidinylmethylamine, which process comprises: i) the reaction of isonipecotamide and 1-bromobutane to give the N-butyl derivative of isonipecotamide; followed by ii) reduction with LiAlH4, characterised in that the reactions i) and ii) are carried out in toluene as solvent.
CN102341397A Improved chemical synthesis of diazaindoles by chichibabin cyclization An improved synthesis method for making diazaindoles using a Chichibabin cyclization is disclosed. In particular, this method is useful for making the compound of Formula I.
EP1583529B9 Amino acid phenoxy ethers, their preparation and uses Novel amino acid phenyl ethers are provided which exhibit activity for the treatment of immunological diseases, inflammation, obesity, hyperlipidemia, hypertension, neurological diseases and diabetes.
US20080287424 e.g. N-[amino(imino)methyl]-2-[2-(4-phenoxyphenyl)-5-phenyl-1H-pyrrol-1-yl]acetamide; beta -amyloid deposits and neurofibrillary tangles; cognition activator, neurodegenerative diseases; Alzheimer's disease, Down's syndrome The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
US20080200521 Novel hydroxamic acid containing amino acid derivatives Novel hydroxamic acid containing amino acid derivatives are provided that are useful for treatment of inflammation, inflammatory and immunological diseases; lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels; and for treatment or prophylaxis of metabolic disorders.
CN103570790A Protopanoxadiol derivative, preparation method of derivative, composition containing derivative and application of composition The invention relates to a protopanoxadiol derivative shown as formula I in the specification, a preparation method of the derivative, a composition containing the derivative and an application of the derivative, and in particular relates to a derivative acquired by modifying protopanoxadiol which is used as a parent structure, a preparation method of the derivative, a composition containing the derivative and an application of the derivative in preparing a tumor cell multi-drug resistance reversal agent.
US20100324043 Bicyclic And Tricyclic Compounds As KAT II Inhibitors Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.
WO2005025581A1 Use of n-acetyl-d-aminoglycosamine in preparation of drugs for the treatment of cacer and metastasis The Use of N-Acetyl-D-Aminoglycosamine in preparation of drugs for the treatment of cacer and metastasis is disclosed in the invention. By modaluting its functions, N-Acetyl-D-Aminoglycosamine can constitute stable parts of the membrane, and involve metabolism process of cancer cells, and lead them to death by stoping energy supply. It has significant effects, as proven by laboratory experiments, animal models and human tests.
US20110112109 Triazolone derivatives A compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen.
US7399485 Rapidly Disintegrable solid preparation A rapidly disintegrable solid preparation which comprises (i) a pharmacologically active ingredient, (ii) a sugar and (iii) a low-substituted hydroxypropylcellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group. The rapidly disintegrable solid preparation has fast disintegrability, suitable strength and no roughness.
CN1883669A Liver-benefiting blood circulation-activating eyesight-improving capsule The invention relates to a capsule for benefiting liver, promoting blood circulation and improving acuity of vision, which comprises the raw materials of gypsum rubrum 90-130g, tabasheer 20-40g, safflower 20-40g, clove 20-40g, chebula fruit 20-40g, belleric terminalia fruit 20-40g, emblic leafflower fruit 20-40g, licorice root 20-40g, multibanded krait 20-40g, herba equiseti hiemalis 20-40g, caraway seeds 20-40g, Meconopsis integrifolia 20-40g, Mumiyah-asil 20-40g, iron powder 60-90g, aragonite 60-90g.
US20120308623 Composition comprising nanoparticles of ti02 The present invention is directed to a composition comprising nanoparticles of TiO2 having a mean particle diameter (D50) of about 20-50 nm at a concentration of about 1-2000 g/L and H2O2 at a final concentration at about 2.5-25% by volume. The TiO2 particles are activated by the H2O2 in the composition to form radicals. The composition has antimicrobial and anti-inflammatory properties and may be used for e.g. wound debridement. The invention further concerns medical and cosmetic products and devices comprising the composition.
US7625894 Pyrrolo[2,3-d]Pyrimidines as Protein Tyrosine Kinase Inhibitors The invention relates to 7H-pyrrolo[2,3-d]-pyrimidine derivatives of formula (I), wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds —for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.
US20090005400 Biologically Active Aphrocallistin Compounds The subject invention provides novel compositions of biologically active compounds which can advantageously be used in blocking cellular proliferation and/or treatment of cancer.
WO2006047228A1 Asymmetric synthesis of substituted dihydrobenzofurans The present invention concerns production of a compound of the formula (I) or a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula (II) where Ar, Y, R1, RY, R2, and m are as defined herein.
CN101804136A External plaster for curing scald and burn sores and preparation method thereof The invention discloses an external plaster for curing scald and burn sores and a preparation method thereof, which belong to the field of medicaments. The preparation method comprises the following steps: removing soil and impurities from frankincense, fossil bone, myrrh, radix pseudo-ginseng, dragon's blood, lead powder and acacia catechu, and sorting the materials; putting the dry materials into a drug roll in proportion for rolling into powder; sieving the powder with a 100-mesh drug sieve and fully mixing the powder; putting sesame oil into an iron kettle in proportion; heating the kettle for 10 to 20 minutes at the temperature of 150 to 200 DEG C; scattering the mixed powder of the seven drugs into the sesame oil with continuous stirring to fully mix the drug powder with the sesame oil; boiling the mixture for 60 to 90 minutes at the temperature of 150 to 200 DEG C; getting the iron kettle away from the flame and pouring the ointment into a metal or high temperature resistant glass container; and placing the ointment at natural temperature until the ointment is cooled for later use. The external plaster has a cure rate of 100 percent for scald, burn and sore, ensures no scar after healing so as to avoid skin grafting for serious scald and burn, ensures that the skin colour of the diseased part restores to the original skin colour by 100 Percent, and has the advantages of having short period of curing, lightening the pain of the patient, avoiding the pain of the skin grafting and reducing the high medical expense.
WO2006032342A3 Carbonyl compound-containing drug and the use thereof The invention relates to the use of the compounds of formula (I), wherein D, E, G, W, X, Y, T, R1 and R2 are defined as in claim 1, in the prophylaxis and/or therapy of thromboembolic diseases.
WO2009001128A1 1,2-cycl0hexane dicarboxamides as cathepsin inhibitors The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.
WO2005063748A1 β-CARBOLINE DERIVED GUANIDINE ALKALOID, TIRUCHENDURAMINE A novel β-carboline guanidine derivative tiruchenduramine (1): and its derivatives are disclosed. These compounds have been isolated from the Indian ascidian Synoicum macroglossum. These compounds are useful in the treatement of diabetic disorder by providing inhibition of α (alpha)-glucosidase.
CN103233055A Preparation method and application of oleanolic 28-O-beta-D-glucopyranoside The invention relates to the field of biological medicaments, in particular relates to oleanolic 28-O-beta-D-glucopyranoside (I) and discloses a preparation method of the oleanolic 28-O-beta-D-glucopyranoside. The oleanolic 28-O-beta-D-glucopyranoside is prepared by carrying out bioconversion on oleanolic acid by using a bacterial strain with the preservation number of NRRL1086. The invention further discloses an application of the oleanolic 28-O-beta-D-glucopyranoside in terms of anti-inflammation.
US20050080045 topical administration; prevention of STDs preferably a viral disease other than HIV, e.g. HPV or genital herpes and especially acyclovir resistant genital herpes There is described a method of treating, alleviating or preventing the transmission of a sexually transmitted disease which comprises the topical administration of dextrin sulphate. There is also described a composition for use in the treatment, alleviation or prevention of a sexually transmitted disease which comprises dextrin sulphates in gel form.
CN101548978A Pharmaceutical composition containing alendronate sodium The invention discloses a pharmaceutical composition containing alendronate sodium and a preparation method thereof. By preparing a solid dispersion, the pharmaceutical composition improves the solubility of the medicament, reduces the irritability of the medicament to the mucous membrane, and increases the bioavailability of the principal medicament and is used for curing osteoporosis.
EP2665492A1 (r)-1,2-propanediol for use as a solvent in therapeutic cooling agent compositions The present invention pertains generally to the field of topical medical therapy, cosmetics, and toiletries. More specifically, the invention relates to the use of a solvent comprising (R)-1,2-propanediol for cooling agents, for example, (R)-2-[((1fl,2S,5R)-2-isopropyl- 5-methyl-cyclohexanecarbonyl)-arnino]-propionic acid n-propyl ester (CPS-410). The invention also relates to cooling agent compositions comprising a cooling agent and,2-propanediol, and methods for their preparation. The invention also relates to the use of such cooling agent compositions in therapy, for example, in the treatment of sensory discomfort, especially sensory discomfort of the skin (e.g., itch). The invention also relates to the use of such cooling agent compositions in cosmetics (e.g., eye make-up products) and toiletries (e.g., after-shave lotion).
CA2722445A1 Nanoemulsions for treating fungal, yeast and mold infections The present invention relates to methods for treating and completely curing fungal, yeast, and/or mold infections in human subjects comprising topically administering to a human subject in need thereof an antifungal nanoemulsion composition.
WO2012131576A1 Pyrrole derivatives as nicotinic acetylcholine receptor modulators for use in the treatment of neurodegenerative disorders such as alzheimer's and parkinson's disease Disclosed is a compound of formula (I) wherein 'a' and R1-R5 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the α7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereofs, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
CN101732271A Dextromethorphan orally disintegrating tablets and preparation method thereof The invention discloses dextromethorphan orally disintegrating tablets and a preparation method thereof. The dextromethorphan orally disintegrating tablets are prepared from the following main raw materials in part by weight: 2 to 8 parts of dextromethorphan, 8 to 12 parts of lactose, 50 to 70 parts of mannitol, 60 to 70 parts of microcrystalline cellulose, 10 to 20 parts of crosslinked PVP, 10 to 20 parts of crosslinked CMC-Na, 2 to 8 parts of Aspartame, 1 to 5 parts of Eudragit E100 and 1 to 5 parts of talcpowder. The method of the invention comprises the following steps: firstly, preparing film-coated granules; secondly, preparing blank granules; finally, uniformly mixing the prepared film-coated granules, the prepared blank granules and additional auxiliary materials in part by weight including 0.1 to 0.3 part of menthol, 1 to 4 parts of magnesium stearate, 10 to 20 parts of 10 to 20 parts of and 2 to 10 parts of essence; and tabletting the mixture and obtaining the dextromethorphan orally disintegrating tablets. The dextromethorphan orally disintegrating tablets of the invention are simple in technical control, fast in absorption, high in bioavailability and convenient in administration.
US20080249164 Antimicrobial and Antinflammatory Composition The invention relates to the use of at least davanone and 1,8-cineol for the manufacture of an antimicrobial and/or antiinflammatory composition as well as a method of producing said composition.
CN103588780A Barium cantharidate and preparation method thereof The invention discloses barium cantharidate. A structural formula (I) of the barium cantharidate is as follows. A preparation method of the barium cantharidate comprises the steps as follows: according to the weight ratio of 1:(30-50), trichloromethane or isopropanol is added into a cantharidin pure product and heated, so that the mixture is dissolved; at the same time, barium hydroxide is added into isometric distilled water of the trichloromethane or the isopropanol, uniform mixing is performed, and the molar ratio of cantharidin to the barium hydroxide is in a range of (3:1)-(3:2); a barium hydroxide solution is added into a trichloromethane solution or an isopropanol solution which dissolves the cantharidin, and magnetic stirring is performed for 6-12 hours; after stirring, the mixture is heated to 60-75 DEG C, and the trichloromethane or the isopropanol is volatilized, so that a white suspension is obtained; the suspension is placed into a drying oven, concentrated and dried, so that white crystal powder is obtained; and according to the weight ratio of (30-50):1, the trichloromethane or the isopropanol is added into the white crystal powder and heated to 40 DEGC, the temperature is kept until the cantharidin is dissolved, then filtering and drying are performed, and white crystal powder is obtained, so that the barium cantharidate is obtained. The barium cantharidate and the preparation method thereof have the characteristics as follows: the antitumor activity is higher, the process is simple, the operation is facilitated, the safety is good, the finished product performance is stable, and the purity is high.
US7569561 For treating carcinoma chosen from cervical, breast, colon, head and neck, lung, pancreas, prostate, sarcomas, leukaemias, lymphomas, melanomas and gliomas The present invention encompasses compounds of general formula (1) wherein R1 to R6, X and Y are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, as well as the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.
US20080260720 Systems and Methods for Inhibiting Metastasis The present invention relates to compositions and methods for cancer therapeutics. In particular, the present invention provides compositions and methods for inhibiting cancer metastasis by inhibiting G12 and G13 activity.
CN103012428A 4-(five-membered heterocycle pyrimidin/substituted pyridine) amino-1H-3-pyrazolecarboxamide CDK (cyclin dependent kinase)/Aurora dual inhibitor and application thereof The invention relates to the field of pharmaceutical chemistry and in particular relates to 4-(five-membered heterocycle pyrimidin/substituted pyridine) amino-1H-3-pyrazolecarboxamide derivatives, preparation methods of the derivatives, medicinal compositions containing the compounds and medicinal applications of the derivatives, especially an anti-tumour application of the derivatives serving as a CDK (cyclin dependent kinase)/Aurora dual inhibitor.
WO2011098746A1 Crystalline acid addition salts of ( 5r) -enanti0mer of pioglitazone A crystalline acid addition salt of 5R-pioglitazone, said salt being selected from the hydrochloride, hydrobromide, (-)-O,O'-dibenzoyl-L-tartrate, phosphate, hydroxy-ethanesulfonic acid and the naphthalene-1,5-disulfonic acid (2:1 ) salts thereof, wherein the naphthalene-1,5-disulfonic acid salt contains 2 molecules of (5R)-5-{4-[2- (5-ethylpyrϊdin-2-yl)ethoxy]benzyI}-1,3-thiazoIidine-2,4-dione for each molecule of naphthalene-1,5-disulfonic acid.
WO2014075554A1 Pharmaceutical composition containing sirolimus esterification and preparation method thereof A Lyophilized pharmaceutical composition and a preparation method thereof. The composition comprises sirolimus esterification and polyethylene glycol stearate 15 as cosolvent.
CN103705514A Composition containing nimodipine, preparation method and application thereof The invention relates to the technical field of calcium antagonist medicines, and discloses a composition containing nimodipine, a preparation method and application thereof. The composition containing nimodipine comprises the following components in mass concentration: 0.02-1 percent of nimodipine, and 0.2-3 percent of surfactant, wherein the pH value of the composition containing nimodipine is in a range of 6.5-8.5. Stimulating ethanol is not adopted in the composition containing nimodipine, so that the dosing risk of the composition containing nimodipine can be reduced, and the stability of the composition containing nimodipine can be improved.
US20110263606 Solid oral dosage forms comprising tadalafil Improved pharmaceutical solid oral dosage forms for the buccal and/or sublingual delivery of Tadalafil. The improved delivery systems for solubilizing and stabilizing pharmaceutically active ingredients exhibit enhanced methods of preparation by the use improved solubilization systems which can maintain the Tadalafil in a buccal and/or sublingual oral dosage form or a polymeric film matrix that provides improved bioavailability and/or absorption of Tadalafil.
CN102988361A Resveratrol and temozolomide double-medicine-loaded nanospheres, as well as application and preparation method thereof The invention discloses resveratrol and temozolomide double-medicine-loaded nanospheres, which are prepared by mixing temozolomide (TEM), resveratrol (RES) and a medicine-loading material, wherein the medicine-loading material is an amphiphilic segmented copolymer, namely, polycaprolactone-polyethyleneglycol (mPEG-PCL) or polylactic acid-polyethyleneglycol (mPEG-PLA) or polyglycolic acid-polyethyleneglycol (mPEG-PLGA) synthesised by polycaprolactone or polylactic acid or polyglycolic acid and polyethyleneglycol. The preparation method comprises the following steps of: dissolving the two raw material constituents, namely, the resveratrol (RES) and the medicine-loading material, in a water-soluble non-toxic organic solvent, and dissolving temozolomide in pure water, and stirring; filtering the obtained light-blue dispersion liquid by a microfiltration membrane having a mesh diameter of 220+30 nm to obtain anti-tumour double-medicine-loaded nanosphere solution having a particle diameter of 80-120 nm; and heat-drying or freeze-drying.
US20080131437 Using allelic variation in cell adhesion molecule (CD164) as tool in treatment and prevntion of skin, arthritic and gastrointestinal disorders The present invention relates to sCD164 variants and therapeutic uses thereof, in particular for treating or preventing inflammatory or autoimmune disorders.
CN101129375B Vinorelbine solid lipid nano granule, freeze drying formulated product and method of preparing the same Disclosed is kind of Vinorelbine solid lipid nanoparticles which comprise (by weight percent) vinorelbine 1-25%, grease material 30-90%, phospholipids 5-50% oleinic acid 0-20%. The preparing process consists of melting liposome material through water-bath, dissolving phosphatides, oleic acid and Vnorelbine with ethanol, dropping into the liposome material, removing ethanol under decompression condition, cooling down and freezing, placing into pH 2-5 aqueous phase, triturating and homogenizing the turbid liquor to obtain the freeze-dried preparation with improved anticancer reactivity of Vinorelbine.
US6998423 Sulfonyl-amino or carbonyl-amino derivatives; osteoporosis bone disorders; therapeutic drug or kits including anti-resorptive agents, anabolic agents; Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
CN1762360A Compound cetirizine hydrochloride gel Disclosed is a cetirizine hydrochloride gelling agent, wherein each 1000g of the gelling agent comprises 100.0g of cetirizine hydrochloride, 0.5-2g of mupirocin, 5.0-10.0g of base, 60-100ml of glycerin propylene glycol, 5.0-10.0g of triethanolamine, right amount of PBS, and balancing distilled water.
CN103446052A Aerosol for treating micro-trauma of human body and using method thereof The invention relates to an aerosol for treating micro-trauma of human body and a using method thereof. The aerosol is prepared by blending wound surface protective agent polyvinyl alcohol, skin sanitizer povidone-iodine or chlorhexidine into aqueous solution by adding distilled water or normal saline, filtering and sterilizing, arranging into a pressure-resistant aerosol tank with a corrosion-resistant coating, wherein the pressure-resistant aerosol tank is provided with a valve comprising a drainage tube, one side of the connection valve, namely the side of the drainage tube of the top end is provided with an opening; pressing the valve and then filling 1.1.1.3,3 perfluoropropane or tetrafluoroethane, installing a nozzle, so as to obtain the aerosol. The using method is as follows: with the distance of 5 to 10centimeters from a cured part, straightly holding the aerosol, continuously pressing and spraying for 5 to 10seconds until the skin is whitened rightly, using repeatedly until the red and swollen and pain of the wound are reduced remarkably. The aerosol has functions in protecting wound surface, preventing and treating infection and relieving swelling and pain, and is especially suitable for the treatment of injury within 24hours. The enough spraying distance can be guaranteed no matter what holding posture the user adopts; therefore the requirement on proper distance of cured part is met.
US20100029658 Heterocyclic derivatives, pharmaceutical compositions and methods of use thereof The present invention relates to novel quinoxaline, quinazoline and phthalazine derivatives as well as multimeric derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds for the treatment and prevention of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in treating and preventing neurodegenerative diseases.
WO2010114476A1 Novel derivatives of steroidal[3,2-c]pyrazole compounds with glucocorticoid activity The present invention provides named compounds of formula (I), and pharmaceutical compositions containing them and their use in therapy.
CN101897711A Pharmaceutical composition containing HMG-CoA reductase inhibitor, aspirin, folic acid and nicotinic acid and applications thereof The invention relates to a lipid-lowering pharmaceutical composition with synergy and the applications thereof. The lipid-lowering pharmaceutical composition with synergy is prepared from one of HMG-CoA reductase inhibitors as medical content, aspirin, folic acid or leucovorin or L-leucovorin and a pharmaceutically acceptable carrier. The pharmaceutical composition has the pharmacological synergy and presents in aspects of reducing blood lipid, preventing atherosclerosis and lowering the risk of cardiovascular accidents. The invention also provides the applications of the pharmaceutical composition to preparing medicines for reducing blood lipid, preventing atherosclerosis and lowering the risk of cardiovascular accidents. Through the implementation of the invention, the pharmaceutical composition providing patients with the special purpose can improve the compliance of patients, is convenient for the patients to take, decreases the medical cost, and has favorable market prospects.
WO2011091892A1 A method for late post coital contraception using ulipristal acetate The invention provides a method for providing post coital contraception in a female subject, comprising providing the subject with a therapeutically effective amount of ulipristal acetate, between about 3 to about 5 days after unprotected intercourse.
WO2008074515A1 Novel hetaryl-phenylene-diamine pyrimidine as protein kinase inhibitors The invention relates to novel hetaryl-phenylene-diamine pyrimidines and the structurally related oxygen and sulfur analogs thereof having the common formula (I). The invention further relates to a method for the production thereof and to the use thereof as a pharmaceutical.
CN103710231A Atractylodes-rhizome healthcare wine for the later period of injury The invention relates to an atractylodes-rhizome healthcare wine for the later period of injury. The healthcare wine is prepared by cleaning 24 parts of atractylodes rhizome, 13 parts of sappan wood, 15 parts of borax, 17 parts of ginger peel, 12 parts of ledebouriella root and 19 parts of acanthopanax bark, drying in the air, smashing into powder, adding the powder into 1 kg of a white sprit having an alcohol content of 54% (v/v), dipping at room temperature for 2-3 months, filtering the dipped materials, and mixing the filtrate with 4 kg of pure-grain alcohol. The preparation method of the healthcare wine is simple. The healthcare wine is convenient to drink and has functions of tonifying the spleen, eliminating dampness, dispelling wind and improving collateral circulation. Drinking of the healthcare wine by the aged can enhance body activity and accelerate body recovery.
WO2007022264A3 Oxides for wound healing and body repair The invention provides a homogeneous composition comprising a hemostatically effective amount of a charged oxide, wherein the composition has an isoelectric point, as measured in calcium chloride, below 7.3 or above 7.4. Typically, the charged oxide is selected from the group consisting of silaceous oxides, titanium oxides, aluminum oxides, calcium oxides, zinc oxides, nickel oxides and iron oxides. In some embodiments, the composition further comprises a second oxide selected from the group consisting of calcium oxide, sodium oxide, magnesium oxide, zinc oxide, phosphorus oxide and alumina. In a typical embodiment of the invention, the charged oxide is silaceous oxide, the second oxide comprises calcium oxide and the ratio, by molar ratio, of silaceous oxide to calcium oxide is 0.25 to 15. Optionally, the composition further comprises phosphorous oxide. Also described are methods of making and using such compositions.
US20090136429 Combination of Anticholinergics and Inhibitors of Phosphodiesterase Type 4 For The Treatment of Respiratory Disease The present invention relates to a combination of an inhaled/oral PDE 4 inhibitor in combination with inhaled anticholinergic bronchodilators (muscarinic receptor antagonists), preferentially Roflumilast or AWD-12-281 and R, R-glycopyrrolate, for symptomatic or prophylactic treatment of respiratory diseases, especially those accompanied by obstruction or inflammation such as chronic obstructive pulmonary disease (COPD) or asthma. It further comprises the presentation of this combination in a locally applied (inhaled) formulation and application in an inhalation device for instance in the Novolizer®.
CN102947289A Arylethynyl derivatives The present invention relates to ethynyl derivatives of formula (I) as allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5). The variables in formula (I) are defined in the specification.
US20100285138 Compositions comprising nanoparticles and apoptotic agents and methods of use Compositions comprising nanoparticles, such as silver or gold nanoparticles or carbon nanotubes (CNTs), and apoptotic agents are described. The nanoparticles can significantly enhance the cancer chemotherapeutic effects of the apoptotic agents. In particular, a highly increased anti-tumor activity has been demonstrated for the combination of etoposide and CNTs against HeLa cells compared to the administration of either etoposide alone or nanoparticles alone. Data provided by flow cytometry, Caspase 3 and other methods, suggest a strong interaction between the nanoparticles and the cellular structure, which can result in the improved effectiveness of chemotherapeutic agents. These findings provide potential new cancer therapies by carefully selecting the right combination of cytostatic drugs and nanostructural materials which synergistically provide significantly greater curative rates.
CN103301078A Lyophilized preparation of D-sodium lansoprazole, and preparation method thereof The invention relates to a lyophilized preparation of D-sodium lansoprazole, and a preparation method thereof. The lyophilized preparation is prepared from D-sodium lansoprazole, mannitol, sodium hydroxide, meglumine and sodium hydrogen phosphate. The defects of low content of the traditional lansoprazole main drug for injection, high impurity and instability of the main drug are overcome by the constituents. The lyophilized preparation is simple in preparation technology; the obtained D-sodium lansoprazole for injection is loose, plump and intact in appearance, good in stability and high in safety, and has development value.
WO2008059141A1 Aminobenzocycloheptene derivatives, methods for preparing the same and uses thereof in therapy The invention relates to a compound of the general formula (I) : F(I) in which: R1, R2, R3, R4, R5, R6, R9, R10, R11 further represent a (C1-C6) alkoxy, (C1-C6) aralkyloxy, (C1-C6) alkylthio, (Q1- C6) aralkylthio radical; R9 et R11 can also form together a carbonated cycle or heterocycle or can form a double bond with the two carbon atoms adjacent to the heptene cycle; R1 et R2 can form together a carbonated cycle or heterocycle; or R1 can be bonded to the heptene cycle by a double bond while R2 is absent; R3, R4, R5 and R6 further represent a polyfluoro (C1-C6) alkyl, (C1-C6) alkoxy radical, an aryl or heteroaryl group; R3 and R4, R4 and R5, R5 and R6 can further form together a methylenedioxy radical joining the adjacent carbon atoms or an aromatic carbonated cycle or an aromatic heterocycle; R7 is a hydrogen atom, a (C1-C6) alkyl radical; X is an oxygen or sulphur atom, N-R12, N-O-R13, in which R12 and R13 represent a hydrogen atom, a (C1-C6) alkyl, (C1- C6) (cycloalkyl) alkyl, (C1-C6) (heterocycloalkyl) alkyl, (C1-C6) aralkyl, (Ci-C6) heteroaralkyl radical; Y is a carbon atom; a nitrogen atom R8 or R9 being then absent; the invention also relates to addition salts with acids except the compound for which R4, R5, R6 represent a methoxy radical, R1, R2, R3, R7 to R11 represent a hydrogen atom, X represents an oxygen atom and Y represents a carbon atom.
CN102153549B Gamma carboline compound as well as preparation method and application thereof The invention relates to a gamma carboline compound as well as a preparation method and application thereof, in particular relates to a histone deacetylase inhibitor based on gamma carboline as a skeleton as well as a preparation method and application thereof. The inhibitor in the invention is a compound having a structural formula as follows (shown in the specification). According to the invention, the synthesis method is simple, the condition is mild, and the compound has high tumor inhibiting rate and is hopeful to become a non-cytotoxins antineoplastic medicament.
WO2010032073A1 Use of opioid antagonists for the preparation of a medicament in the treatment of retinal degenerative diseases Retinal degenerative diseases affect the delicate layer of retina tissue that lines the inside back of the eye leading to gradual vision loss. The use of opioid anatgonists for the preparation of a medicament for the selective blocking of the body' s opioid receptors sites is a method of treating this human suffering by daily administration to the patient of from about 0,5 to about 10 mg of drugs such as naltrexone, naloxone or nalmefene. They act primarily by normalizing derangements in the human complement system that may occur in the disease etiology. Therapeutical approach for macular degeneration and retinitis pigmentosa is primarily intended. Oral, parenteral uses as well as topical applications may all be considered. They may be administered in one or divided doses daily for the best receptor blocking activity, preferably in the evening hours. Low Dose Naltrexone suitable for oral administration is most preferred regimen at about 4.5 mg / day.
US20080268051 Anti-angiogenesis; viscosity inducing component is injectable into the vitreous of a mammalian eye without permanently diminishing visual acuity Anti-angiogenesis compositions, and methods of using such compositions, useful for injection into the vitreous of human eyes are provided. Such compositions include MAAC solutions or particles present in a therapeutically effective amount, a viscosity-inducing component, and an aqueous carrier component. The compositions have viscosities at about 25° C. of at least about 10 cps or about 100 cps at a shear rate of 0.1/second. In a preferred embodiment, the viscosity at 25° C. is in the range of from about 80,000 cps to about 300,000 cps.
WO2007058482A1 Novel inhibitors of protein kinase The present invention relates to novel compounds for inhibition of angiogenesis receptor tyrosine kinases, in particular, VEGF receptor 2 kinase ('KDR') activity, and preparations for preparation of them, and the use of them, and pharmaceutical compositions containing them at a therapeutically effective amount. The compounds according to the present invention are useful for the treatment and prevention of diseases resulting from the undesired KDR activity, for example, angiogenesis-related diseases such as cancers, psoriasis, rheumatoid arthritis, diabetic retinopathy, etc.
US20130023502 Substituted pyridinyl-pyrimidines and their use as medicaments The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
US20120329760 Rnase 7 as a marker for infection Methods of identifying a subject having a urinary tract infection using RNase 7 are described. The methods include providing a test sample of urine from the subject, determining the level of RNase 7 in the test sample, and then comparing the level of RNase 7 in the test sample to the level of RNase 7 in a control. A higher level of RNase 7 in the test sample indicates that the subject has an acute urinary tract infection, whereas a lower level of RNase 7 in the test sample indicates that the subject only has a chronic urinary tract infection.
WO2010054042A3 Dimethylphenoxy modulators of viral protease activity and/or parasitic enzyme activity The present invention relates to new dimethylphenoxy inhibitors of viral protease or parasitic enzymes, pharmaceutical compositions thereof, and methods of use thereof. Formula (I)
US20080227845 Cyclooxygenase-2 inhibitor/histone deacetylase inhibitor combination The invention relates to a combination which comprises (a) a cyclooxygenase-2 inhibitor (“COX-2 inhibitor”) and (b) a histone deacetylase inhibitor (“HDAI”) for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of pre-malignant colon lesions or a colon cancer or other malignancies in a mammal, particularly a human. The invention also relates to pharmaceutical compositions comprising such a combination and to a method of treating pre-malignant colon lesions (e.g. polyps) and colon cancer, as well as other malignancies, in a mammal, particularly a human, with such a combination. The present invention further also relates to a commercial package or product comprising such a combination.
US7553823 C-pyrazole A2A receptor agonists 2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
US20110190343 Hiv-1 fusion inhibitors and methods A new series of HIV-1 fusion inhibitors and methods of use are disclosed. The compounds are based on a substituted indole, benzimidazole, indoline or isoindoline fragment. The compounds find use in inhibiting or preventing HIV fusion from occurring, thus inhibiting or preventing entry of viral RNA into host cells. The compounds may be useful towards other biological targets involving protein-protein interactions.
WO2014157860A1 Process for the preparation of high purity olanzapine and crystalline form ii thereof The present invention provides a process for the preparation of high-purity olanzapine with high yield and a process for the preparation of olanzapine crystalline Form II, which are industrially applicable. The preparation processes according to the present invention are useful for the preparation of high-purity olanzapine and olanzapine crystalline Form II with high yield and thus can be effectively used for mass production.
WO2013156231A1 Use of imidazotriazinones in neuropathic pain Provided herein are compounds for use in the treatment of neuropathic pain and the neuropathic pain syndromes, in particular the use of imidazotriazinones. Pharmaceutical compositions, single unit dosage forms, and kit suitable for use for the treatment of neuropathic pain and the neuropathic pain syndromes are also disclosed.
US20120225937 Crystalline forms and processes for the preparation of pg12 receptor agonists The present invention relates to salts of 2-(2-((4-(((4-chlorophenyl)(phenyl)-carbamoyloxy)methyl)cyclohexyl)methoxy)acetamido)ethanesulfonic acid (Compound 1) and crystalline forms, solvates and hydrates thereof. The present invention further relates to processes and intermediates useful in the preparation of Compound I and salts, solvates and hydrates thereof. Crystalline forms, salts, solvates and hydrates of the present invention and pharmaceutical compositions thereof are useful in the treatment of for example, pulmonary arterial hypertension (PAH); platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; atherosclerosis; acne; type I diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).
CN102440981A Application of natural resveratrol dimer Pallidol-like compound in pharmacy The invention belongs to the technical field of pharmaceutical chemistry and pharmaceutical technology, and relates to new application of a natural resveratrol dimmer Pallidol-type compound with a structure of a format (I) in pharmacy, in particular to antioxidation of the natural resveratrol dimmer Pallidol-type compound. According to the invention, through an HUVEC (human umbilical vein endothelial cell) pharmacological test in vitro, the result shows that the natural resveratrol dimer can remarkably improve cell viability and cell protection vitality, and has good dosage dependence to the potential protection function of oxidative stress injury, and obvious antioxidant. The natural resveratrol dimmer Pallidol-type compound can be as a drug for curing cardiovascular diseases, and is further prepared into various preparations which contain the natural resveratrol with safe and effective quantity and drug carriers.
US20070293450 Identification of ses-3 and the uses of same The invention relates to isolated nucleic acid molecules coding for SES-3 proteins or muted SES-3 proteins, and vectors and transgenic organisms containing such nucleic acid molecules. The invention also relates to uses of such nucleic acid molecules or others which are functionally similar, for producing pharmaceuticals and for producing model organisms. The invention further relates to the corresponding SES-3 proteins and muted SES-3 proteins, and the antibodies induced thereby. Finally, the invention relates to the use of substances which increase the expression of human presenilin, for the treatment of Alzheimer's disease, in addition to said substances themselves and pharmaceutical compositions containing the same.
EP1712237A2 Erythropoietin solution preparation stabilized with leucine, glutamic acid or lysine This invention provides an erythropoietin solution preparation containing an amino acid as a stabilizer, and having excellent long-term storage stability.
WO2005009421A2 The use of 1-amino-alkylcyclohexane compounds in the treatment of pain hypersensitivity The invention relates to a novel use of 1-amino-alkylcyclohexane NMDA receptor antagonists such as neramexane in the treatment of pain hypersensitivity and neuropathic pain.
EP2651922A1 Indoles as respiratory syncytial virus antiviral agents Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
CN103083303A Application of salvianolic acid A composition in preparing medicines for improving neural function symptom after cerebral ischemia The invention relates to application of a salvianolic acid A composition in preparing medicines for improving neural function symptom after cerebral ischemia. The composition is prepared from the following components in percentage by weight: 90-99% of salvianolic acid A, 0.1-3% of alkannic acid, 0.1-3% of rosmarinic acid, 0.1-3% of salvianolic acid B and 0.1-5% of salvianolic acid C.
CN101235047A Rare earth complex, preparation method and antibiotic application of the same The invention discloses a naphthoic acid and 1, 10-o-phenanthroline rare-earth complex and relative function for inhibiting bacterial, which is represented as REL3phen.nH2O, wherein RE is rare-earth element as Eu3+, Tb3+, Gd3+, La3+ or Y3+, L is alpha-Naphthoic acid, beta-Naphthoic acid, alpha-Naphthlcetic acid or beta-Naphthlcetic acid, n=0 or 1. The preparation method comprises using L as first ligand and o-phenanthroline as second ligand while RE3+: L: phen is 1:3:1, adding alcohol and dissolving, mixing the two ligands to be added into a rare-earth chloride solution, mixing and reacting to synthesize rare-earth complex. The qualitative and quantitative bacteriostatic tests of filter paper method on the rare-earth complex prove that the rare-earth complex has bacteriostatic function on variable experimental bacteria, stronger than independent ligand and ion and stronger bacteriostatic effect along with density increase. The invention provides useful try for biological bacteria inhibitor development.
WO2013150993A1 Pharmaceutical for preventing or treating gingivitis [Problem] The present invention addresses the problem of providing an excellent pharmaceutical for preventing gingivitis or treating gingivitis. [Solution] The present invention provides a pharmaceutical for preventing or treating gingivitis, the pharmaceutical having as an active ingredient a hydantoin derivative represented by general formula (I) (in the formula, X signifies a halogen atom or hydrogen atom, and R1 and R2 either simultaneously or separately represent a hydrogen atom or optionally substituted C1-6 alkyl group) or a pharmaceutically acceptable salt thereof.
US20060058325 Therapeutic quniazoline derivatives Quinazoline derivatives of formula (I): wherein A is 6-membered heteroaryl containing a nitrogen atom and optionally containing one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.
CN1579408A Medicine for spasmolysis and relieving pain and preparation method The invention is a spasmolysis and pain easing medicine and its manufacturing method, it extracts medicine active substance enoxolone glycyrrhetinic acid from liquorice and extracts active substance paeoniflorin from peony according to the curing mechanism of peony and liquorice. And then are blended with medicine carrier and/or excepient, thus the current medicine with the same curative effect to peony and liquorice soup can be produced; it has a small volume, convenient, and has no toxin and side effects.
US20100021386 Treatment, prevention,and reversal of alcohol-induced liver disease This invention relates to methods for treating, preventing, or reversing liver disease or damage produced by chronic alcohol intake by administering at least one peroxisome proliferator activated receptor (PPAR) agonist.
CN102805735A Esomeprazole enteric pellet tablets and preparation method thereof The invention relates to a preparation method for esomeprazole enteric pellet tablets. The method comprises the following steps of: preparing esomeprazole enteric pellets, and preparing mixed tablets of the pellets and excipient; the esomeprazole enteric pellets contain active pharmaceutical pellet cores, isolation layers and enteric coatings; the esomeprazole enteric pellets prepared by the method have certain elasticity and are pressureproof; the esomeprazole enteric pellets and the excipient are pressed to form tablets, so that the pellets can be isolated from air, and are more stable than pellet capsules; the validity period can reach over three years; and the esomeprazole enteric pellet tablets have the advantages of small size, dividable dose and the like, and the compliance of a patient is improved.
US20090076168 Amine-based and imine-based polymers, uses and preparation thereof The present invention relates to a modified polysaccharide prepared from the reaction between a polysaccharide comprising a plurality of monosaccharide subunits having at least one primary amino group, and an hydrophobic aldehyde. The aldehyde and the amino group form together an imine or amine group. The process for preparation and use in cosmetic, pharmaceutical and food industry of the modified polysaccharide is also disclosed.
WO2009115517A3 Pyridines and pyrazines as inhibitors of pi3k The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar', A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.
CN102697708A Ropivacaine hydrochloride injection and preparation process thereof The invention discloses formula components and a preparation process of ropivacaine hydrochloride injection. The preparation process comprises the steps of: (1) weighing raw and auxiliary materials according to the formula; (2) mixing the raw and auxiliary materials, standing and filtering; (3) measuring and regulating the pH value of the solution; (4) filtering medicine liquid by 0.45mum and 0.22mum microporous filter membranes; (5) encapsulating the medicine liquid while introducing N2; and (6) and carrying out sterilization. The product obtained according to the preparation process disclosed by the invention meets the national requirements of 'notice about issuing the basic technical requirements on chemical injection and multi-component biochemical injection' and the national quality standard of the medicine.
CN102367251A More stable tropisetron compound and pharmaceutical composition thereof The invention relates to a more stable tropisetron compound and a pharmaceutical composition thereof. According to the invention, a tropisetron crude product is recrystallized for 1-3 times with ethyl acetate and acetone the ratio of which is 1:1 and decoloring is carried out with activated carbon so as to obtain white-like crystals.
US7253161 Cognition activators; neurodegenerative disease; anxiolytic agents; Alzheimer's diseas; Pick's disease; schizophrenia; psychological disorders; antiischemic agents; antiepileptic agents; antidepressants Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or halogen, their isomers and also their addition salts. Medicaments.
CN102584805A Preparation method of one new active ingredient in natural plant The invention provides a preparation method of separating and purifying a new active ingredient from a natural plant-safflower aeschynanthus acuminatus. The preparation method is characterized in that a new compound is separated and purified from the safflower aeschynanthus acuminatus by traditional extraction and chromatographic separation technologies. The preparation method comprises the following steps: extracting by cold soaking, concentrating by flash distillation, separating by column chromatography and the like, and separating from the safflower aeschynanthus acuminatus to obtain the new compound: 5,7-dyhydroxy-8-C-beta-D-glucose chromone carbon glycoside, wherein the extraction rate of the compound is 1.1% and the purity of the compound is above 96%. The preparation method is simpler, economic, safe, high-yield and unpolluted. A preliminary activity research shows that the prepared compound has certain effects of bacterial inhibition and oxidation resistance, and has good prospects of development and application.
CN103524442A Pyrimidine compound, triazine compound and application thereof as medicine The invention relates to substituent pyrimidine and (1, 3, 5)-triazine derivatives, which have wide therapeutic use by inhibiting one or more protein kinase. A compound with a chemical formula I, pharmaceutical salt or solvate, and physiologically hydrolyzable, solubilized or fixable derivatives are shown in the specification, wherein Ar is an optional substituent group shown in the specification, and is a quinary heteroaromatic ring or a hexahydric aromatic ring; R is an optional substituent group including H, CH3, SONH2, Pz, MePz, AcPz, Dz, MeDz, AcDz, M, PzC, PzS and MePzS; Y is N, Z is NH, and Ar is a thiazole-5-group. The invention also provides a preparation process of the compound, a pharmaceutical composition containing the compound, a purpose of the compound and a use method of the compound and the composition in treatment of different diseases.
US20070032528 inhibitors of vascular endothelial growth factor receptor tyrosine kinase; antiproliferative agents; antitumor; 4-Hydroxy-3-(5-methylbenzimidazol-2-yl)hydropyridino[3,4-b]pyridin-2-one; nitrogen containing cyclic compounds Organic compounds having the structural formula I are provided where the variables have the values described herein and R1 and R2 join together to form a 6 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group. Pharmaceutical formulations include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
EP1497268A2 Nitric oxide donors, compositions and methods of use The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating inflammation, pain, fever, gastrointestinal disorders, respiratory disorders and sexual dysfunctions. The nitric oxide donors donate, transfer or release nitric oxide, and/or elevate endogenous levels of endothelium-derived relaxing factor, and/or stimulate endogenous synthesis of nitric oxide and/or are substrates for nitric oxide synthase and are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The therapeutic agent can optionally be substituted with at least one NO and/or NO2 group (i.e., nitrosylated and/or nitrosated). The invention also provides novel compositions and kits comprising at least one nitric oxide donor and/or at least one therapeutic agent.
WO2006075955A1 Pyrazolyl acylsulfonamide derivatives as endothelin converting enzyme inhibitors and useful in the treatment of chronic obstructive pulmonary disease The invention provides compounds of formula (I),wherein R1,R2 ,R3 and R4 are as defined in the specification,processes for preparing such compounds,to pharmaceutical compositions comprising such compounds and to the use of the compounds as active therapeutic agents (F).
CN101716166A Applications of 2', 4'-dihydroxyl-6'-methoxyl-3', 5'-dimethyl chalcone The invention relates to applications of 2', 4'-dihydroxyl-6'-methoxyl-3', 5'-dimethyl chalcone the preparations of medicines, foods or health care products for inhibiting alpha-glucosaccharase activity, also relates to the application of the 2',4'-dihydroxyl-6'-methoxyl-3',5'-dimethyl chalcone to the preparations of medicines, foods or health care products with a hypoglycemic function, and also relates to the application of the 2',4'-dihydroxyl-6'-methoxyl-3',5'-dimethyl chalcone to the preparations of medicines, foods or health care products for treating or preventing diabetes and complications thereof. Therefore, through the invention, the 2',4'-dihydroxyl-6'-methoxyl-3',5'-dimethyl chalcone can be used for preparing the medicines, the foods or the health care products for inhibiting the alpha-glucosaccharase activity, lowering blood sugar, and treating or preventing the diabetes and the complications thereof, and brings relief for diabetics.
CN101405285A Cyclic-alkylaminederivatives as inhibitors of the interaction between MDM2 and P53 The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R<1> , R<2> , R<3>, R<4>, R<5>, R<6>, R<7>, Q, Y and Z have defined meanings.
EP1418891B1 Anaesthetic formulations of propofol Propofol solubilised in aqueous micellar preparations of poloxamers and containing local anaesthetic is associated with reduced levels of pain on injection.
US20120114702 Compositions and methods for treating asthma and other lung disorders Provided are compositions and methods for treating lung or respiratory disorders or conditions characterized by airflow obstruction or limitation, or symptoms thereof (e g, asthma, rhinitis, allergic rhinitis, and chronic obstructive pulmonary disease (CaPO) and CaPO-associated conditions (e g, bronchitis, emphysema, asthma), emphysema, pneumonia, bronchitis, in-fluenza, SARS, tuberculosis, and whooping cough (pertussis), and the like) comprising administering a therapeutic composition comprising at least one electrokinetically altered fluid comprising an ionic aqueous solution of charge-stabilized oxygen containing nanostructures as disclosed herein, or comprising administering a nonelectrokinetic superoxygenated aqueous solution The methods preferably comprise regulating intracellular signal transduction by modulation of at least one of cellular membranes, membrane potential, membrane proteins (e g, membrane receptors, (e g, G protein-coupled receptors, and intercellular junctions)) Additional aspects include therapeutic compositions, and combination treatment methods comprising administration of electrokinetically generated fluid in combination with at least one additional therapeutic agent (e g, albuterol, etc).
US20120270803 Mitotic Kinesin Inhibitors and Methods of Use Thereof This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
US20080031971 Use Of Xenon For The Prevention Of Programmed Cell Death Described is the use of xenon for preventing or reducing cellular death, preferably aberrant apoptosis. Preferred embodiments relate to the use of xenon for preventing (a) cellular damage for tissue and organs to be transplanted, (b) apoptotic cell death after eye laser surgery, and (c) for protecting endothelial cells of the intestine in sepsis.
CN103356484A Magnetic solid "dextran-MLDH-fluorouracil" liposome The invention relates to a magnetic solid "dextran-MLDH-fluorouracil" liposome. The liposome is characterized in that: dextran-MLDH-fluorouracil is taken as the drug carrier, soya lecithin and cholesterol are taken as the raw materials, then the dextran-MLDH-fluorouracil liposome is prepared through the film-dispersion method, the reverse-evaporating method or the ethanol-injection method, mannitol is added into the liposome and then subjected to a freeze-sublimation treatment, and finally the product is obtained. The liposome completely maintains the crystal structure and morphology features of DMF, and has a prominent "lipid bilayer-DMF" core-shell structure characteristic and stable properties. The product is water-soluble solid magnetic liposome, and has the advantages of typical in-vitro controlled releasing performance, sensitive magnetic responsiveness, excellent cancer cell proliferation activity inhibiting ability and special and long in-vivo drug process. The invention provides an effect method for preserving DMF liposome. The method is suitable for preparation and curing preservation of magnetic drug liposome, which takes magnetic layered compound hydroxide MLDH as the carrier, has the processing advantages of low cost and simple preparation, and has the characteristics of integration of magnetic targeting and controlled releasing functions, long and durative effects, stable curative effects, and convenient storage and transportation.
WO2013117693A1 Pde4 inhibitor for treating huntington's disease Use of a compound of formula (I): 5-{5-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-1,3,4-oxadiazol-2-yl}-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine (I) or a pharmaceutically acceptable salt thereof for the treatment of Huntington's disease.
WO2004070012A3 Cell-killing molecules and methods of use thereof The invention provides compositions comprising amino acid sequences that have cell killing activity, nucleic acid sequences encoding them, antibodies that specifically bind with them, and methods of using these compositions for increasing and/or reducing cell death, detecting cell death, diagnosing diseases associated with altered cell death, and methods for identifying test agents that alter cell death.
CN102702044A Carbocyclic and heterocyclic arylsulfones as gamma secretase inhibitors This invention discloses carbocyclic and heterocyclic arylsulfones compound as gamma secretase inhibitors. The compound is formula (IF) compound and can be used for treating Alzheimer's disease.
US20120149759 Treatment of insulin gene (ins) related diseases by inhibition of natural antisense transcript to an insulin gene (ins) The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of an Insulin gene (INS), in particular, by targeting natural antisense polynucleotides of an Insulin gene (INS). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of Insulin Gene (INS).
CN102716077A Sitafloxacin auristilla and preparation method thereof The invention discloses a sitafloxacin auristilla. The auristilla takes sitafloxacin and borneol as the main ingredient, and takes acetic acid and grain alcohol (75 percent) as auxiliary material. The invention further discloses the preparation method of sitafloxacin auristilla. The medicine provided by the invention is the fourth generation carbostyril synthetic antibacterial agents, is highly active in antibacterium and has a direct and enduring effect. With the auxiliary of borneol, the auxiliary effects of reducing swelling and alleviating pain are achieved, and the compliance of patients can be improved. Meanwhile, the invention meets the requirements of novel medicine for curing ear infection diseases clinically.
WO2011159067A3 Thiazole derivatives as sglt2 inhibitors and pharmaceutical composition comprising same The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.
CN101647788B Florfenicol microcapsule and preparation method thereof The invention discloses a florfenicol microcapsule which is prepared by the following method: (1) preparing a gelatin solution from gelatin, glycerin and distilled water; (2) adding the gelatin solution prepared in the step (1) in florfenicol, grinding and dripping an acetate solution and a sodium sulfate solution; (3) cooling and then adding a formaldehyde solution and a sodium hydroxide solution; (4) standing for delamination, removing supernatant liquid, performing suction filtration, washing with water, and finally drying in reduced pressure vacuum at 50 DEG C to 60 DEG C. A simple coacervation method is adopted to prepare the florfenicol microcapsule and the method has the advantages of simple process, high encapsulation rate reaching 80 percent to 85 percent, and strong operability.The florfenicol microcapsule prepared by the method can cover the bitter taste of florfenicol drugs, improve the stability of drugs and reduce the stimulation to animal stomaches, thereby being better applied to the treatment of animal diseases, laying a foundation for developing a new florfenicol excipient and bringing economic benefits for society.
US7674455 treating a mammal having amyotrophic lateral sclerosis by transducing a motor neuron of the mammal with an insulin-like growth factor I (IGF-1) gene or a glial cell line-derived neurotrophic factor (GDNF) gene; neurodegenerative disorders Methods are disclosed for delivering a heterologous gene to a cell body of a neuron by contacting a muscle tissue innervated by the neuron with a viral vector comprising a heterologous gene, wherein the viral vector enters said neuron and is retrogradely moved to the cell body. Additionally, methods for expressing secreted proteins from a nerve cell body as well as methods for treating neurodegenerative disorders such as amyotrophic lateral sclerosis are described.
US6897201 Administering a nucleoside 5'-pyrophosphate pyranoside or analogue, of given formula The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a nucleoside 5′-pyrophosphate pyranoside or analogue, which is defined by general Formula I. The method of the present invention is useful in the treatment or prevention of ocular hypertension, such as found in glaucoma, including primary and secondary glaucoma. The method can be used alone to reduce intraocular pressure. The method can also be used in conjunction with another therapeutic agent or adjunctive therapy commonly used to treat glaucoma to enhance the therapeutic effect of reducing the intraocular pressure. The present invention also provides a novel composition comprising a nucleoside 5′-pyrophosphate pyranoside or analogues.
DE102010042360A1 Nasal spray bottle, useful for dilution of drug to be administered, and for preventing or treating rhinitis medicamentosa, preferably withdrawal rhinitis medicamentosa, comprises a spray nozzle and a two chamber system Nasal spray bottle, for dilution of drug to be administered, comprises a spray nozzle (1) and a two chamber system, where the two chambers are connected by a vertical wall and the first chamber (2) a nasal spray containing active ingredient (3) and the second chamber (4) contains a diluent (5). - ACTIVITY : Antiallergic; Antiinflammatory. - MECHANISM OF ACTION : None given.
WO2014016789A1 Pyrazolo[3,4-d]pyrimidin-4(5h)-one derivatives as pde9 inhibitors A compound of the general formula (I) wherein R1 is selected from the group consisting of phenyl unsubstituted or substituted with 1 to 3 substituents selected from F, Cl, Br, I, CN, -O-C1-C3-alkyl, fluorinated -O-C1-C3-alkyl, -(CH2)mOH and 5-membered heterocyclic group with 1 or 2 heteroatoms selected from N, O and S; and 6- or 10-membered heteroaryl with 1 to 3 heteroatoms selected from O, N and S; R2 and R3 independently of each other represent H atom or straight or branched C1-C3 alkyl; R4 is selected from the group consisting of 4- to 6- membered cycloalkyl, wherein one of carbon atoms can be replaced by O atom, and which is unsubstituted or substituted with one or two halogen atoms,and straight or branched C1-C4 alkyl; Q represents a bond or C1-C3-alkylene, which can be optionally substituted by one to three C1-C3-alkyls; X is selected from the group consisting of O, NR5, and S(O)p; R5 represents H atom or C1-C3alkyl; m is 1, 2 or 3; p is 0, 1 or 2; and salts thereof, for use as a medicament, in particular for treating cognitive function disorders and neurodegenerative diseases.
EP2382873A1 Novel use of organic compound The present invention is directed to the use of a compound selected from the group consisting of β-carotene, lutein, lycopene and β-cryptoxanthin, and mixtures thereof with CoQ-I O for maintaining the energy metabolism, the energy flow and/or the energy production in skin or of skin of animals including humans, for maintaining the respiratory function of the skin of animals including humans, for energizing the skin, maintaining and supporting the radiance and natural glow of the skin of animals including humans and for promoting a healthy appearance of the skin of animals including humans for preventing UV-A radiation-inducted mtDNA mutagenesis in skin of animals including humans, as well as for the manufacture of a composition, preferably an orally applicable composition, for these uses and the corresponding methods. The present invention is further directed to the use of a compound selected from the group consisting of β-carotene, lutein, lycopene, and β-cryptoxanthin, and mixtures thereof and combinations thereof with CoQ-10 in sunscreens as well as daily care products to improve their photoprotective potential, as well as to their use as effective micronutrients for skin maintenance. Furthermore the present invention is directed to compositions, preferably orally applicable compositions, comprising a certain amount of at least one compound selected from the group consisting of β-carotene, lutein, lycopene and β-cryptoxanthin and mixtures thereof and combinations thereof with CoQ-10 as active ingredient, characterized in that the amount is effective for such uses as mentioned above.
US7582288 Methods of targeting multiple cytokines The invention relates to protein complexes and fusion proteins including at least two different cytokine molecules. The protein complexes and fusion proteins may further include a targeting moiety such as a region of an immunoglobulin. Methods of using the protein complexes and fusion proteins are also disclosed.
CN101773617A Drug for treatment of asthmatic bronchitis The invention discloses a drug for treatment of asthmatic bronchitis, which is prepared by taking ephedra, almond mud, gypsum, caulis perillae, platycodon, couchgrass root, green forsythia and cortex moutan radicis as raw materials. The invention has good use effect, accurate curative effect and the effective rate of over 65%.
WO2012022707A1 Substituted heteroaryl spiropyrrolidine mdm2 antagonists There are provided compounds of the general formula (I) wherein A, B, V, W, R1, R2, R3, R3, and R4, are as described herein, enantiomers and pharmaceutically acceptable salts thereof, as well as methods for making said compounds and pharmaceutical compositions containing them. The present compounds are useful as anticancer agents, in particular as agents in the therapeutic and/or prophylactic treatment of solid tumors such as for example breast, colon, lung and prostate tumors.
WO2011109217A3 Methods of treating or preventing rna polymerase dependent viral disorders by administration of jak2 kinase inhibitors The present invention is directed to methods of treating or preventing RNA polymerase dependent viral disorders using JAK2 kinase inhibitors or agents that inhibit HEXIM1 tyrosine phosphorylation. In a particular aspect the present invention is directed to the treatment of prevention of HIV infection in a subject by administration of JAK2 kinase inhibitors or agents that inhibit HEXIM1 tyrosine phosphorylation.
CN102631322A 20 (S)-protopanoxadiol dry suspension agent and preparation method thereof The invention relates to a 20 (S)-protopanoxadiol dry suspension agent and a preparation method of the 20 (S)-protopanoxadiol dry suspension agent. The 20 (S)-protopanoxadiol dry suspension agent takes 20 (S)-protopanoxadiol as active ingredient, and the mass ratio between the active ingredient and pharmaceutic adjuvant is 1-20%: 80-99%; and the pharmaceutic adjuvant comprises suspending agent and wetting agent with the mass ratio of 5: 1, or sweetener with the mass ratio of 0-5%. The preparation method of the 20 (S)-protopanoxadiol dry suspension agent comprises the steps of: weighing the suspending agent and the wetting agent according to the prescription dosage, and then leading the suspending agent and the wetting agent to be evenly mixed with the 20 (S)-protopanoxadiol, or adding the sweetener. The 20 (S)-protopanoxadiol dry suspension agent is rapid to absorb and high in bioavailability, and overcomes the defect that tablets, capsules and the like are difficult to take, thus especially suitable for children and elderly patients; meanwhile, the preparation method is simple and high in industrial applicability.
CN103479589A Cefpodoxime proxetil dispersible tablet and preparation method thereof The invention discloses a cefpodoxime proxetil dispersible tablet which comprises the following raw materials in percentage by weight: 20-45 percent of cefpodoxime proxetil, 30-50 percent of filler, 5-15 percent of a disintegrating agent, 0.25-1.0 percent of a wetting agent, 0.25-1.5 percent of a flavoring agent and 5.0-15 percent of polyethylene glycol 200. The preparation method adopts a specific wetting agent, so as to improve mobility, dissolubility and uniformity in mixing of the product and facilitate the storage of the product, and after the product is stored for a period of time, no obvious changes occur. According to the invention, the cefpodoxime proxetil dispersible tablet is obtained through direct powder mixing, granulation and tabletting, and the preparation method is simple without any special equipment, and is suitable for industrial production.
EP1134222B1 IMIDAZO[4,5-b]PYRIDINIUMMETHYL-CONTAINING CEPHEM COMPOUNDS HAVING BROAD ANTIBACTERIAL SPECTRUM Cephem compounds represented by general formula (I) which have a broad antibacterial spectrum over various pathogenic bacteria and are also efficacious against MRSA, wherein X represents N or CY (wherein Y represents H or halogeno); R1 represents optionally protected amino; R2 represents hydrogen, optionally substituted lower alkyl, etc.; R3 represents hydrogen, etc.; R4 represents hydrogen, optionally substituted lower alkyl, an optionally substituted nitrogen-containing heterocycle, etc.; R5 represents hydrogen, etc.; and the wavy lines means syn- or anti-isomerism or a mixture thereof.
WO2013110590A1 Substituted phenylimidazopyrazoles and use thereof The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives of the fomula (I), to processes for preparation thereof, to the use thereof for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially of angiogenic disorders and hyperproliferative disorders where neovascularization is involved, for example cancers and tumors. Such treatments can be effected as a monotherapy or else in combination with other medicaments or further therapeutic measures.
CN102743398A Dexamethasone sodium phosphate composition The invention relates to a dexamethasone sodium phosphate, which is prepared by a spray-drying method, and contains the following auxiliary materials by calculating the composition containing 1g of dexamethasone sodium phosphate: 0-100g of excipient, 0.01-59g of disodium hydrogen phosphate and 0-0.5g of sodium dihydrogen phosphate.
CN102793684A Roflumilast liquid preparation and preparation method thereof The invention relates to a roflumilast liquid preparation. The preparation comprises a medicinal active component, a diluent and a solvent, wherein the medicinal active component is roflumilast; every 1,000 the liquid preparation particles comprise 0.3 to 0.8g of roflumilast and 150 to 300g of diluent. The liquid preparation is prepared from roflumilast, so the problem that uniformity of roflumilast in a conventional preparation is poor can be solved, and a roflumilast liquid preparation with good uniformity is provided.
CN103239403A Preparation and storage method of vincristine sulfate liposome The present invention discloses a novel vincristine sulfate liposome composition formulation for intravenous injection and a preparation method and a storage method thereof. The invention belongs to the field of pharmaceutical preparations, and relates to vincristine sulfate liposome and a preparation method and a storage method thereof. The vincristine sulfate liposome of the present invention is formed by vincristine sulfate and at least one phospholipid, and can include at least a surfactant or a cryoprotectant or cholesterol. The storage method includes room temperature storage, cold storage, frozen storage and frozen dry storage. The pharmaceutical preparation is stable, is high in encapsulation rate, has no drug penetration phenomenon, is low in burst release rate, is simple and reliable in the specific preparation method, and is conducive to industrial production.
US20110046137 Pyrazole Derivatives as P2X7 Modulators The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The pyrazole derivatives of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.
CN1899286A Racanisodamine eye drops The present invention discloses one kind of racanisodamine eye drops, which consist of water for injection in 100 ml, racanisodamine in 0.051-0.999g, sodium hyaluronate in 0.012-0.049g, and isoosmotic regulating agent 0.4-2.5g. The racanisodamine eye drops have obvious curative effect on near sightness. Animal experiment proves less irritation on eye and stable performance. The racanisodamine eye has small dosage and low cost.
CN1723882A Medicine composition of sublingual application or on-cheek or in nasal-cavity A composite medicine for treating ejaculation praecox by applying it under tongue or to buccal or nose cavity contains the depressant of pentahydroxy tryptamine, medicinal salt and medicinal auxiliaries. Its advantage is quickly taken its high curative.
WO2009128964A2 Ensemble-based virtual screening reveals novel antiviral compounds for avian influenza neuraminidase The embodiments provide compound that can bind to the avian influenza virus subtype H5N1 neuraminidase protein, as well as compositions, including pharmaceutical compositions comprising a subject compound. The embodiments further provide treatment methods, including methods of treating avian influenza.
WO2014006020A1 Gpbp-1 inhibition and its therapeutic use The present invention provides compositions including anti-tumor agents and inhibitors of Goodpasture antigen binding protein, p21, and ABCC7, and their use in treating cancer.
US8044031 Method for increasing the survival of aquatic and other animals exposed to an aquatic virus, birnavirus or other RNA virus and composition for such methods A method of increasing the survival of animals and aquatic species susceptible to birnavirus infection by treating them before, during and/or after birnavirus exposure, with a chemical compound capable of inhibiting viral replication. A method of treating aquatic species to increase their survival in the presence of a virus, particularly an aquatic birnavirus, and to increase the yield of farmed fish susceptible to viral infection. The present invention provides methods for increasing survival of virally-exposed aquatic animals by administering therapeutically effective amounts of aminoghycoside compounds to aquatic animals susceptible to birnavirus infection and/or IPNV infection, particularly in fish such as salmonoid species, which are easily exposed to IPNV. The present invention also provides methods for increasing survival of virally-exposed animals by administering therapeutically effective amounts of aminoghycoside compounds to farmed animals susceptible to birnavirus infection and/or IBDV infection, particularly in poultry such as chickens, which are exposed to IBDV.
CN101967113A 3-alloc amido-3-(3- nitryl-4-fluorophenyl) propionic acid and preparation method thereof The invention relates to a 3-alloc amido-3-(3- nitryl-4-fluorophenyl) propionic acid and a preparation method thereof. The method comprises the following steps of: (1) generating 3-nitryl-4-fluorobenzaldehyde by reacting 4-fluorobenzaldehyde under the action of concentrated sulfuric acid and concentrated nitric acid; (2) refluxing the 3-nitryl-4-fluorobenzaldehyde, malonic acid and ammonium acetate in an alcoholic solvent for 6-8 h to obtain 3-amido-3-(3- nitryl-4-fluorophenyl) propionic acid; and (3) mixing the 3-amido-3-(3- nitryl-4-fluorophenyl) propionic acid with 8-12% sodium carbonate solution in percentage by weight and dioxane to form a suspension, adding a AllocCl and dioxane solution to the suspension and reacting to generate 3-alloc amido-3-(3- nitryl-4-fluorophenyl) propionic acid. A series of peptide compounds obtained by synthesizing the 3-alloc amido-3-(3-nitryl-4-fluorophenyl) propionic acid with other amino acids have a certain inhibitory activity on HDAC (Histone Deacetylase). The invention has the advantages of simple preparation method, easily obtained raw materials and high yield.
CN101113149B Aliphatic organic acid salt of berberine type alkaloid and preparation method and usage thereof The invention relates to preparation method and application of berberine fatty group organic acid salt, pertaining to pharmacy field. The chemical general formula of barberine type alkaline of the invention is shown as a formula (I), wherein, X represents organic acid group, and the berberine type alkaline is berberin, palmatine, jaterohitine or coptisine. The invention relates berberine alkalinefatty group organic acid, which is of good oral taking absorption, can be used for preparing medical components, greatly improves the bio-availability of the alkaline type, and play comparatively better effect to the therapies of such diseases as bacterial infection, heart rate abnormity, platelet aggregation, hyperlipidemia, diabetes, hypertension, cardiac failure, etc.
US20080020994 G proteins in tumor growth and angiogenesis The invention provides an agent that reduces the expression of Gα12 or Gα13 polypeptide, as well as an agent that enhances G protein Gα12 or Gα13 expression and/or activity. An agent of the invention may be used to decrease or increase G protein Gα12 or Gα13 expression and/or activity thereby to treat or prevent the onset of a disease or condition associated with Gα12 or Gα13 expression and/or activity. The invention also provides a method for screening for an anti-cancer or anti-angiogenesis agent, as well as an agent that promotes angiogenesis.
CN103172619A 4-(substituted benzyl)-1(2H)-2,3-phthalazinone derivatives, and preparation methods, medicinal compositions and uses thereof The invention relates to 4-(substituted benzyl)-1(2H)-2,3-phthalazinone derivatives, and preparation methods, medicinal compositions and uses thereof, and concretely relates to compounds of formula I or isomers thereof, and pharmaceutically acceptable salts, solvates, chemical protection types and prodrugs thereof. R1, R2, R3, R4, R5 and R6 in the formula I are defined in the specification and the claim in the invention. The compounds are effective poly(ADP-ribose)polymerase (PARP) inhibitors.
US20120020886 Thermal spin cross-over compounds and methods of using same A compound has the of Formula I or a salt thereof: Such compounds may be used to image cells, tissues, organs, fluids, or a subject. Such compounds may also be used in pharmaceutical compositions.
CN100596280C Film for treating oral ulcer and preparation method thereof The invention discloses a plastering film for treating ulcerative stomatitis and its preparation, wherein the medicament is prepared from honeysuckle flower, menthol, vitamin B2, boneol, tetracaine hydrochloride, sorbic acid, prednisone acetate, chlortetracycline hydrochloride, glycerin, stevioside, ethanol, polyvinyl alcohol PVA17-88 and purified water.
CN103263428A Application of polyflavanostilbene A in preparation of anti-tuberculosis bacteria medicaments The invention discloses an application of polyflavanostilbene A in preparation of anti-tuberculosis bacteria medicaments. The invention is designed against the current situation that the incidence rate and the mortality rate of tuberculosis are in a rising trend due to high incidence rate of the tuberculosis and the appearance of multiple-resistant strains of tuberculosis bacteria and finds that the polyflavanostilbene A has significant inhibition activity against the tuberculosis bacteria and further has good application prospects. The use of the polyflavanostilbene A in the preparation of the anti-tuberculosis bacteria medicaments, disclosed by the invention, belongs to the first disclosure, as the framework type belongs to the brand new framework type, the strong inhibition activity against the tuberculosis bacteria is unexpected, the possibility of giving any notices by other compounds does not exist, and the polyflavanostilbene A has prominent substantial characteristics; and simultaneously, the polyflavanostilbene A obviously has a significant progress in control of infection of the tuberculosis bacteria.
CN103142588A Amoxicillin sodium sulbactam sodium for injection and preparation method of amoxicillin sodium sulbactam sodium The invention relates to amoxicillin sodium sulbactam sodium for injection for livestock and a preparation method of the amoxicillin sodium sulbactam sodium. The invention aims at providing an amoxicillin sodium sulbactam sodium freeze-dried powder injection. The amoxicillin sodium sulbactam sodium freeze-dried powder injection comprises effective components of amoxicillin sodium and sulbactam sodium, and also contains an antioxygen, a pH(Potential Of Hydrogen) regulating agent and a dispersing agent, and thus the solubility of the amoxicillin sodium is greatly increased, and the pH of medicine liquid after being re-dissolved is within a range of 8.5-9.5. According to the amoxicillin sodium sulbactam sodium and the preparation method of the amoxicillin sodium sulbactam sodium, through research of the preparation of an amoxicillin sodium sulbactam sodium stock solution and determination of a freeze-drying process, the amoxicillin sodium sulbactam sodium freeze-dried powder injection which is stable in quality, better in appearance characteristics and safe and effective in use is obtained.
US7015017 Process and agent for instabilizing viral quasi-species-distributions avoiding resistance phenomena A process for instabilizing viral quasi-species-distributions under avoidance of resistance phenomena by replication of the nucleic acids of the viruses present in the quasi-species-distribution by of a defective replication system, a) whereby the defective replication system has a rate of misincorporation for nucleotides above the rate of misincorporation of the viral wild-type-replication system and, whereby the viruses are replicated by the replication system having the higher rate of misincorporation at least as effectively as it is done by the replication system of the wild-type virus, b) and/or negative influence of the replication of the consensus-sequence (nucleic acid sequence of the wild-type virus) in relation to other replicatable nucleic acids.
US8772288 Substituted spiro[cycloalkyl-1,3′-indo]-2′(1′H)-one derivatives and their use as P38 mitogen-activated kinase inhibitors The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
CN101036633A Enteric coated omeprazole pellets capsule and the preparing method thereof The invention relates to an omeprazole enteric micropill capsule and a process for preparing the same. The content of the capsule is omeprazole enteric micropill including a blank pill core; an activity medicine layer having an alkaline component; a separator containing magnesia and titanium pigment; and an enteric coat layer. According to synergistic reaction, stability of the medicine is distinctly improved. The omeprazole enteric micropill capsule of the invention has period of validity of the preparation to three years or more.
US20080021106 Cellular uptake of bioactive agents Provided is a composition and a method for increasing cellular uptake of bioactive agents, particularly those compounds termed “small molecules” into the cells of mammalian tissue, such as the epithelial cells of the mucosa.
WO2014061821A1 Grb10 interacting gyf protein 2 modulator A GIGYF2 modulator including, as an active ingredient, a compound represented by the following Formula (I): wherein, in Formula (I), R1 and R2 each independently represent a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms, or R1 and R2 may bind together to form a cyclic group with a nitrogen atom attached thereto; and n represents an integer from 2 to 6.
WO2008082542A1 Combination of vitamin k and vitamin k antagonist such as r-isomer of warfarin, phenprocoumon or r-isomer of phenprocoumon as anticoagulant therapy Medications which are derived by combining one or more doses of the agonist, vitamin K, with doses of one or more selected vitamin K antagonists such as the R-isomer of warfarin, the R-isomer of phenprocoumon, or the racemic phenprocoumon are useful in anticoagulant therapy. These products are designed to minimize or circumvent the detrimental impact of newly identified genetic-based variables that currently significantly complicate the therapeutic response of individual patients to anticoagulation therapy.
CN101732549A Cough liquid and preparation method thereof The invention discloses cough liquid and a preparation method thereof. The main therapeutic functions of the medicament include dispelling wind, abating fever and dissipating heat, relieving cough and reducing sputum and diminishing inflammation and nourishing lungs. According to the formula of the cough liquid, every 500 grams of the cough liquid comprises 18 to 23 grams of bulbus fritilariae, 27 to 32 grams of moxa, and 140 to 160 grams of rock candy. The cough liquid is obtained through mixing fresh moxa liquid and bulbus fritilariae powder, rock candy and water and then sealing the mixture for 2 to 3 months. The preparation method comprises the following steps: removing the stalks of fresh moxa and removing moisture after cleaning and sunning; then, mashing the moxa and extruding liquid for later use; crushing bulbus fritilariae into 80 to 100-mesh powder; boiling water and adding rock candy in the boiled water; adding bulbus fritilariae powder and moxa liquid after cooling the boiled water and bottling the mixture after stirring; and finally, sealing the mixture for 2 to 3 months to obtain the cough liquid.
CN102961353A Glipizide sustained-release dropping pill for treating diabetes and preparation method thereof The invention belongs to the technical field of pharmacy, and in particular relates to a glipizide sustained-release dropping pill for treating diabetes and a preparation method thereof. Based on glipizide sustained-release dropping pill, the drug provided by the invention is prepared by existing preparation technology of dropping pill. Compared to the prior art, the invention is the supplement for the defects of existing drug form production, and provides a drug, which has advantages of high bioavailability, rapid effectiveness, long-acting effect, little toxic or side effect, high drug content, small and accurate dosage, convenient usage, low price and convenience for carrying.
WO2008080134A3 4-amin0-2- (hetero) arylamino-5- (hetero) arylthiazoles useful as axl inhibitors Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.
US20060094013 Salt-inducible kinases 2 and use thereof The polypeptide of the present invention has the amino acid sequence represented by SEQ ID NO: 2, 4, 6, 8, 10, or 12. The polypeptide of the present invention is useful as an agent for preventing or improving a disease with which the metabolic disorder of fat cells or the like is associated.
US20120022153 Tricyclic condensed heterocyclic compound, process of producing same, and use thereof A novel compound derived from the culture product of an actinomycete and having an antitumor activity is provided. Provided is a compound represented by any one of formulas (I), (II) and (III) or an optical isomer thereof or a pharmaceutically acceptable salt thereof which can be isolated from the culture fluid of an actinomycete which belongs to the genus Streptomyces, wherein R1, R2, R5 and R6 each independently represent a hydrogen atom, a methyl group, a hydroxymethyl group, a hydroxyl group, or a double bond by which R1 and R2 or R5 and R6 are bonded; R3, R4, R7 and R8 each independently represent a methyl group or a hydroxymethyl group; and R9 represents a hydrogen atom or a hydroxyl group.
WO2013093615A1 Tricyclic boron compounds for antimicrobial therapy Provided herein are antimicrobial tricyclic boron compounds of the following formula I: or pharmaceutically acceptable salts, complexes, or tautomers thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
EP2785706A1 Substituted 4 - phenyl - pyridines for the treatment of nk-1 receptor related diseases Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NKj) receptor. The compounds have the general formula (I):
US20130109644 Methods for treating cancers using oral formulations of cytidine analogs Provided herein are methods for treating subjects having a cancer, such as a relapsed or refractory solid tumor, wherein the method comprises administering to the subject a cytidine analog. In certain of the methods, the cytidine analog is administered alone or in combination with one or more anti-cancer agents. Also provided are methods for using a cytidine analog, to treat diseases and disorders including disorders related to abnormal cell proliferation, hematologic disorders, and immune disorders, among others. In certain of the methods, the cytidine analog is formulated in an oral dosage form and administered orally.
US20060264437 Azabicyclylmethyl derivatives of 2,3-dihydro-1,4-dioxino [2,3-F]quinoline as 5-HT1A antagonists Compounds of the formula are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia, and are also useful for the treatment of disorders such as anxiety, aggression and stress, and for the control of various physiological phenomena, such eating disorders, disorders of thermoregulation, and sleep and sexual dysfunction.
US20110092470 Method of treating men with erectile dysfunction A method of treating male sexual dysfunction or erectile dysfunction by administration of a 5alpha reductase inhibitor together with a testosterone supplement is described. The method is also concerned with the use of the 5alpha reductase inhibiting compound and the testosterone supplement together with another agent useful for treating erectile dysfunction, including PDE V inhibitors; AGE (advanced glycation end-product) breakers; alpha 1 blockers; alpha 1A antagonists; alpha 2 antagonists; dopamine agonists; dopamine D4 agonists; melanocortin agonists; oxytocin agonists; prostaglandin; radical scavengers; rotamase inhibitors; aviptadil; nitroglycerine; and GPCR agonists for treating male sexual dysfunction or erectile dysfunction.
CA2545723A1 Use of cathepsin k inhibitors in severe bone loss diseases This invention relates generally to cathepsin K inhibitors and their use in bone growth. Specifically, the invention relates to the use of cathepsin K inhibitors to stimulate new bone formation in patients in need thereof.
EP0918514B9 Triaryl methane compounds for the treatment of cancer, actinic keratosis and kaposi's sarcoma The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. The compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.
WO2014028322A1 Modulators of the histamine h3 receptor and the treatment of disorders related thereto The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders.
CN102240290A Pharmaceutical composition containing prulifloxacin, and preparation method thereof The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing prulifloxacin, and a preparation method thereof. The pharmaceutical composition is characterized by containing prulifloxacin and a pharmaceutically acceptable carrier, wherein the pharmaceutically acceptable carrier at least comprises phosphate, and the weight ratio of the prulifloxacin to the phosphate is (1:2)-(2:1). Shown by stability tests, the impurity content of the pharmaceutical composition provided by the invention is obviously lower than that of a common preparation.
WO2012097750A1 Pyrazolopyrimidinone compound and imidazo-triazone compound for treating erectile dysfunction Disclosed are selective phosphodiesterase inhibitor compounds shown in formula (I) or (II) for treating Erectile Dysfunction, the pharmaceutically acceptable salts and configurational isomers thereof. In the formula, the substituents R1, R2, R3, R4 and R5 are defined as in the specification. Also disclosed are a medical composition comprising compounds of formula (I) or (II), and the use of these compounds for preparing a drug treating or preventing male Erectile Dysfunction.
US7803562 Method for screening human intestinal Npt2B modulatory agents A novel human sodium phosphate cotransporter expressed on the apical surface of intestinal epithelial cells (huNpt2B) and polypeptides related thereto, as well as nucleic acid compositions encoding the same, are provided. The subject polypeptides and nucleic acid compositions find use in a variety of applications, including research, diagnostic, and therapeutic agent screening applications. Also provided are methods of inhibiting Npt2B activity in a host and methods of treating disease conditions associated with Npt2B activity.
CN103030713A Preparation method of low-molecular-weight glucan-niacin polymer with hypolipidemic activity The invention discloses a preparation method of a low-molecular-weight glucan-niacin polymer with a hypolipidemic activity and belongs to the field of biological chemistry. The preparation method comprises the following steps: activating beta-glucan 2,000 by an activating agent such as epoxy chloropropane, and coupling the activated beta-glucan 2,000 with niacin and niacin derivative methoxypyrazine. The mice test results show that the polymer has significant hypoglycemic capability. The preparation method is easy to operate, low in cost, low in environment pollution and suitable for large-scale application.
US20110312890 Acetylated amino acids as anti-platelet agents, nutritional and vitamin supplements This invention relates to pharmaceutical compounds and nutritional supplements that are acetylated derivatives of naturally occurring amino acids and acetylated derivatives of peptides derived from naturally occurring amino acids containing hydroxyl groups. They are as useful as anti-platelet drugs, and as nutritional supplements.
US20120252789 Inhibitors of sphingosine kinase The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
US6883516 Preparing solution of first component in liquid component such that after volatilization of liquid by passing solution through flow passage while heating, aerosol is formed having predetermined particle size distribution of first component A method is provided for generating an aerosol. The method includes preparing a solution formed of a first component in a liquid component such that after volatilization of the liquid component by passing the solution through a flow passage while heating the solution, an aerosol is formed having a predetermined particle size distribution of the first component, wherein the solution is prepared such that the amount of the first component therein is sufficient to achieve the predetermined particle size distribution of the first component. The method also includes passing the solution through the flow passage while heating the solution to a temperature sufficient to volatilize the liquid component, wherein the flow passage comprises an outlet through which the first component and the volatilized liquid component flow, and wherein an aerosol is formed.
US20120264753 Novel 1-(biphenyl-4-yl-methyl)-1h-imidazole derivative and pharmaceutical product containing same Disclosed is a novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative represented by general formula (I), which has both angiotensin II receptor antagonist activity and PPAR-γ activating activity and is useful as a prophylactic and/or therapeutic agent for cardiovascular diseases and metabolic diseases. Also disclosed is a pharmaceutical composition which contains the novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative. In general formula (I), ring A represents a group represented by formula (II) or (III); R1 represents a C1-6 alkyl group; R2 represents a C1-6 alkyl group which may be substituted by a hydroxy group, or a group represented by formula —CO—R4 (wherein R4 represents a hydroxy group, a C1-6 alkoxy group, an amino group, a mono(C1-6 alkyl)amino group, a di(C1-6 alkyl)amino group, a morpholino group, a piperidino group or a pyrrolidino group); R3 represents a halogen atom or a C1-6 alkoxy group; and X and Y may be the same or different and each represents a nitrogen atom or CH.
US20080166438 Chromones As Therapeutic Agents The present invention describes the identification and isolation of chromones and novel chromone compositions from plant sources that exhibit up-regulation of adiponectin production by adipocytes and the normalization of virtually hundreds of genes related to glucose and fatty acid metabolic and signaling pathways. The chromone compositions are effective in enhancing adiponectin production by adipocytes and regulating genes involved in fatty acid biosynthesis, mitochondrial β-oxidation of fatty acids, steroid biosynthesis, gluconeogenesis, fat transport, PPARα/RXRα liver signaling and xenobiotic metabolism. The chromone compositions can be used to increase insulin sensitivity, improve glucose tolerance, lower triglyceride levels and balance glucose levels in mammals. Included in the present invention are methods for the prevention and treatment of a variety of diseases and conditions including, but not limited to insulin resistance, glucose intolerance, hyperglycemia, metabolic syndromes, dyslipidemia, and hypertriglyceridemia.
WO2008006969A3 Novel tetracyclic derivatives, process for the preparation thereof and pharmaceutical compositions which contain them Compounds of formula (I): in which: > R1, R2 and R3, as described in the description, form a ring of formula (II) where R6 is a hydrogen or halogen atom, or an alkyl, alkoxy, amino, alkylamino or dialkylamino group, and X is a hydrogen atom or an N-OR7 group, > R4 and R5 are a hydrogen or halogen atom, or an alkyl, alkoxy, alkylamino or dialkylamino group, > A is as defined in the description, > B is an alkyl or alkenyl group substituted with a [-CHR8R9 group.
US20100233225 Method of surface coating devices to incorporate bioactive molecules A first embodiment is a coating for a surface comprising an electrostatic self-assembly creating one or more coating layer(s); (i) wherein one or more high molecular weight bioactive molecule(s) is bound to a protein carrier wherein said protein carrier or said bound bioactive molecule is further bound to one or more of said coating layer(s) and/or (ii) wherein one or more low molecular weight bioactive molecule(s) is/are incorporated within one or more of said layers or later introduced to said layer or layers by post-treatment. A second embodiment is a method of coating a surface comprising introducing said surface into a solution of one or more positively charged water-soluble polyelectrolytes at a pH ranging from about 2 to about 12 and at a temperature ranging from about 4° C. to about 80° C. and incubating said surface for about 0.5 to about 60 minutes; Rinsing said surface with said buffer solution or water to remove weakly bound material on said surface and dry by means known to one skilled in the art; Introducing said surface into a solution of one or more negatively charged water-soluble polyelectrolytes at a pH ranging from about 2 to about 12 and at a temperature ranging from about 4° C. to about 80° C. and incubating said surface for about 0.5 to about 60 minutes; and Rinsing said surface with said buffer solution or water to remove weakly bound material on said surface and passively or actively drying said surface.
CN1623545A Glasqiong hydrochloride oral disintegrating tablet and its preparation method An oral disintegrating tablet of Gelasiqiong hydrochloride for treating vomiting is prepared from Gelasiqiong hydrochloride, flavouring agent and disintegrant.
CN101822650B Minocycline hydrochloride sustained release tablet and preparation method thereof The invention relates to a minocycline hydrochloride sustained release tablet and a preparation method thereof. In the technical scheme, the minocycline hydrochloride sustained release tablet is composed of a tablet core and a film coat, the tablet core is composed of minocycline hydrochloride, a sustained release material, a bonding agent, a filling agent and a lubricating agent, the film coat is composed of a film forming material, in the preparation method, the granule is manufactured by means of the high shear wet method and obtained through the drying of a boiling bed, the temperature ofthe material dried by a fluidized bed is controlled to be 25-35 DEG C, and the moisture content of the granule is controlled to be 2.0-4.0 percent. The invention belongs to the technical field of pharmaceutical preparation, which aims to provide an available preparation process for the minocycline hydrochloride sustained release tablet and greatly reduce the relevant materials introduced druing the preparation by controlling the key parameters in the preparation process. The preparation method of the minocycline hydrochloride sustained release tablet and the method for controlling of the relevant materials aim to develop a sustained release formulation of minocycline hydrochloride, and various specifications can be issued based on the body weight of a patient, thereby reducing the peak valley fluctuation of the blood concentration, effectively controlling the adverse drug reaction, and improving the drug bioavailability.
EP1303277B1 Pharmaceutical composition based on cocaethylene and use thereof for treating psychoactive substance dependence The invention concerns a pharmaceutical composition containing cocaethylene as active ingredient and its use for treating psychoactive substance dependence, in particular cocaine.
US20060134249 proanthocyanidin from hops; detoxification a toxicity from germs causing infectious disease Proteotoxin neutralizers containing as the active ingredient proanthocyanidins obtained from hop.
EP0836613B1 Water-soluble adenosine kinase inhibitors This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo[2,3-d] pyrimidine and 3-aryl pyrazolo[3,4-d] pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these and other adenosine kinase inhibitors in the treatment of cardiovascular and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.
US20110218218 Formulations Of Indanylamines And The Use Thereof As Local Anesthetics And As Medication For Chronic Pain Internal-dermal formulations of RS—, S—, or R-2-[2-(N-phenyl-N-2-indanyl)aminoethyl]piperidine causing intradermal accumulation of said piperidine and intended for the treatment of neuropathic pain are provided, as well as a method of inducing the relief of pain using the compounds.
CN102872254A Granules for activating blood and removing stasis The invention discloses granules for activating blood and removing stasis, which are characterized by comprising the following raw materials: semen persicae preparata, rheum officinale, ramulus cinnamomi, radix glycyrrhizae preparata, mirabilite, radix paeoniae rubra, radix angelicae sinensis, radix rehmanniae, cortex moutan radicis, flos carthami and sappanwood.
US20090022823 Methods for Administering Active Agents to CYP3A4 Sensitive Patients The present invention relates, in part, to the discovery that parenterally administered extended release formulations possess an unexpected advantage in treating patients possessing active CYP 3A4. This advantage is particularly beneficial where the individual is concomitantly administering a CYP 3A4 inhibitor or is in risk of doing so. Thus, the invention relates to a method for treating individuals possessing a functional CYP3A4 gene with an active agent metabolized by CYP3A4 comprising parenterally administering the active agent in a first extended release formulation in a first administration and the formulations for use in such methods. The invention further includes a method for preventing adverse drug reactions in individuals possessing a functional CYP3A4 gene with an active agent metabolized by CYP3A4 comprising parenterally administering the active agent in a first extended release formulation in a first administration.
CN102228485A Composition for burn rehabilitation and preparation method thereof The invention provides a composition for burn rehabilitation and a preparation method thereof. The composition comprises pine needle and pharmaceutical excipients. The composition has remarkable effects of treating scars, pigmentation and the like of burned patients, and can remarkably remove scars, pigmentation and the like caused by burns to ensure that the skin of the patients is basically recovered.
CN102309563A Medicinal preparation used for treating diarrhoea of livestock and poultry The invention discloses a medicinal preparation used for protecting the livestock and poultry from diarrhea, which comprises the following raw materials by weight ratio: 1-20 parts of Radix Astragali, 1-20 parts of bighead atractylodes rhizome, 1-20 parts of licorice, 2-40 parts of white peony root, 20-150 parts of Limonite, 20-150 parts of red halloysite, 2-20 parts of pomegranate rind, 20-100 parts of alum, 3-30 parts of radix bupleuri, 4-10 parts of cimicifuga foetida, 1-20 parts of coptis and 0-3 parts of diphenoxylate. The components of the medicinal preparation are direct and mutual synergism, and has efficacy of supplementing the center and boosting qi, lifting up Yang and depression, antidarrhea with astringent, inhibiting smooth muscle spasm of gastrointestinal tract and alleviating peristaltic of gastrointestinal tract, and is capable of rapidly recovering the functions of gastrointestinal tract, thereby, the medicinal preparation has an obvious function of weight increasing.
US8314126 Disubstituted phenylpiperdines/piperazines as modulators of dopamine neurotransmission The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho,meta-disubstituted phenyl)-1-alkypiperidines and piperazines. wherein R1, R2, R3 and X are as defined.
US6929790 Containing a zinc compound containing free available zinc ion and at least one stabilized oxidation potential raising compound, stored separately and mixed prior to using the oral composition. The present invention relates to an oral composition containing a zinc compound containing free available zinc ion and at least one stabilized or stable Eh raising compound distributed in an oral vehicle. The present invention further relates to a method of inhibiting the formation of sulfur containing anions and preventing a reduction in the Eh of the oral cavity. A method of reducing oral malodor and gingivitis and periodontitis is also provided by this invention.
US20110275696 Thioxanthone-Based Autophagy Inhibitor Therapies to Treat Cancer The present specification provides compositions comprising a thioxanthone-based autophagy inhibitor and/or a cancer therapeutic autophagy inducing compound, pharmaceutical kits comprising these compositions, and methods of treating cancer using such compounds, compositions and kits. Additionally, the present specification provides methods of treating cancer using a thioxanthone-based autophagy inhibitor and a radiotherapy.
CN102228430A Nano-suspension for silybin-phospholipid complex and preparation method thereof The invention discloses a nano-suspension for a silybin-phospholipid complex and a preparation method thereof, wherein the nano-suspension for a silybin-phospholipid complex is prepared by combining a technology of promoting medicine absorption by a phospholipid complex with a solubilizing-targeting technology of nano-suspension; the ingredients of the nano-suspension for silybin-phospholipid complex comprise a silybin-phospholipid complex, a stabilizer and water; the nano-suspension exists in the form of suspension or freeze-dried powder and prepared by combining a microprecipitation method with a high-pressure homogenization method; the method of the invention prepares a nano-suspension hard to dissolve in a medicine, without a need to pre-micronize raw material medicines, which greatly decreases energy consumption; the grain diameter distribution range of the prepared nano-grains is narrow, and the medicine highly disperses in a granular state, which increases the wettability, solubility and solution velocity of the medicine, thereby improving the oral bioavailability thereof; the technique process of the preparation method is simple and easy to realize industrial production.
CN101579407A Method for preparing animal models with low serum melatonin level by using acidoid The invention belongs to the technical field of experimental animals and aims at solves a technical problem in providing a method for constructing animal models with low serum melatonin level. The technical proposal of the invention is that each animal orally takes 10.0-100.0 ml/Kg.d of lavage acidoid and molding is carried out for 5-15 days. The method has simple steps, can successfully and repeatedly construct the animal models with continuously-low serum melatonin level and has good application prospect.
CA2254561C Method of producing dry thioctic acid The present invention is relative to a method of producing dry thioctic acid in which a raw material in which concentrated thioctic acid is present is treated with liquid or supercritical CO2, thus yielding thioctic acid with low residual solvent contents in a simple industrial method.
WO2011076019A1 Mixed compound medicament of natural medicine component and no donator and use thereof The present invention discloses a mixed compound medicament of natural medicine component and NO donator. Said medicament consists of at least one natural medicine component and at least one NO donator by mixing at any ratio of mass concentrations. The natural medicine component is anti-tumor medicinal material, and the NO donator is the compound which is able to release NO. The mixed compound medicament of the present invention can effectively enhance the anti-tumor activity and selectivity of natural medicine component, avoid the toxicity and adverse effect of non-natural medicine component, as well as exert the anti-tumor activity of NO. Therefore said medicament has the significant double effect on inhibiting the activity of pathological cells and can be used for treating cancer widely and effectively.
WO2008054748A3 Indazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto Indazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia) Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
US8808725 Solid forms for tissue repair This invention provides coral-based scaffolds for cartilage repair, and instruments for insertion and utilization of same within a site of cartilage repair.
CN1844122A Benzoporphyrin chlorophyll photosensitizer and its preparation process and use The invention relates to a group of novel chlorine family photosensitizer of benzoporphyrin compounds, the method for preparation and use thereof. The compounds have a general formula (I), wherein R1 represents H, CH3, CO2CH3, CH2CO2CH3, CHCO2CH3, R2 represents COOCH3, CO, when R2 is CO, R1 is CHCOOCH3, R3 represents H, low level alkyl, (CH2)mOH, (CH2)mNR4R5, R4 and R5 separately represent low grade alkyl, m represents an integer in the range of 2-6, the low grade alkyl means C1-6 straight chain or branched chain alkyl.
CN103087050A Aryl kinase inhibitor The invention belongs to the technical field of medicines, in particular to an aryl kinase inhibitor represented by the general formula (I), pharmaceutically acceptable salts or stereisomers thereof, wherein R1, R2, R3, m, n, R5, Y, W, M, L or Q are defined in the specification. The invention further relates to a preparation method of the compounds, pharmaceutical preparations or pharmaceutical compositions comprising the compounds, and an application of the compounds for preparing medicines for treating and/or preventing ALK or c-Met mediated cancer related diseases.
CN103536921A Application of cholesterol metabolite for inhibiting liver cancer growth The invention relates to application of cholesterol metabolite for inhibiting liver cancer growth. Particularly, the cholesterol metabolite has the effect of inhibiting growth of a liver cancer cell; the growth of the liver cancer cell can be inhibited by accumulation of the cholesterol metabolite; the inhibition effect can be relieved by excretion of the cholesterol metabolite; expression of an acetyl-coa acetyl transferase (ACAT2) gene in a liver cancer tissue is associated with accumulation of the cholesterol metabolite.
CN102813925A Application of carbon monoxide releasing molecules in preparing medicines for inhibiting blood coagulation activation diseases The invention discloses application of carbon monoxide releasing molecules in preparing medicines for inhibiting blood coagulation activation diseases. In vivo animal experiments and in vitro cell experiments show that exogenous carbon monoxide can significantly reduce the expression of blood coagulation factors FIB and D-D in sepsis, and reduce the expression of platelet membrane glycoprotein CD 61 and CD 62p in plasma, thereby down-regulating the adhesiveness and aggregation function of platelet, inhibiting the phosphorylation level of platelet HIS of sepsis mice and finally inhibiting over activation of the coagulation system in sepsis. When the carbon monoxide releasing molecules are adopted for inhibiting over activation diseases of the coagulation system in sepsis, the concentration control is relatively easy and accurate, adding is convenient for long-term use, and the requirement of clinical application can be satisfied.
US20120015050 Methods and materials for assessing loss of heterozygosity This document provides methods and materials involved in assessing samples (e.g., cancer cells) for the presence of a loss of heterozygosity (LOH) signature. For example, methods and materials for determining whether or not a cell (e.g., a cancer cell) contains an LOH signature are provided. Materials and methods for identifying cells (e.g., cancer cells) having a deficiency in homology directed repair (HDR) as well as materials and methods for identifying cancer patients likely to respond to a particular cancer treatment regimen also are provided.
US20120071859 Inducible interleukin-12 The invention provides an isolated or purified nucleic acid comprising a nucleotide sequence encoding a nuclear factor of activated T-cells (NFAT) promoter operatively associated with a nucleotide sequence encoding IL-12. The invention also provides a nucleic acid comprising a nucleotide sequence encoding a nuclear factor of activated T-cells (NFAT) promoter operatively associated with a nucleotide sequence encoding IL-12, wherein the NFAT promoter is located 3′ of the nucleotide sequence encoding IL-12. Also provided are related recombinant expression vectors, host cells, populations of cells, and pharmaceutical compositions. The invention further provides the use of the inventive nucleic acids or related materials in the treatment or prevention of cancer or an infectious disease in a mammal and in the induction of IL-12 expression in a mammal.
CN102988682A Oral liquid for tonifying kidney and spleen and preventing and treating osteoporosis The invention provides oral liquid for tonifying kidney and spleen and preventing and treating osteoporosis. Concentrated decoction comprising the following components in parts by weight: 8 to 15 parts of astragalus, 8 to 12 parts of codonopsis pilosula, 8 to 12 parts of fried bighead atractylodes rhizome, and 8 to 12 parts of fried yam contains 30 to 60 weight parts of chondroitin sulfate. The invention also provides the oral liquid for tonifying kidney and spleen and preventing and treating osteoporosis, which is characterized by comprising the following components in every 100 parts of water: 10 to 50 parts of the oral liquid, 10 to 30 parts of honey, 0.01 to 0.03 part of sodium alginate, and proper natural edible essence. The product has good effect of preventing and treating osteoporosis.
US7348318 α-Amino-N-(diaminophosphinyl)lactam derivatives There are disclosed a novel α-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH2)n— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.
CN1839899A Liver disease-treating medicine Disclosed is a preparation for treating hepatic diseases, which is preared from Penthorum chinese Pursh and at least one selected from the following constituents: ammonium glycyrrhizinato, glycine, DL-methionine, tiopronin, Lamivudine, and Lovastatin.
WO2011129371A1 GENE GROUP CAPABLE OF ENHANCING ANTI-TUMOR EFFECT OF 5-FU ALONE OR IFN-α/5-FU COMBINATION A group of genes which can enhance the anti-tumor effect of 5-fluorouracil are found. Disclosed is an enhancer of the sensitivity to 5-fluorouracil, which comprises a nucleotide fragment encoding at least one gene selected from the group consisting of PRAKG2 gene, TGFBR2 gene and EXT1 gene.
EP2078719A1 Compound having bicyclic pyrimidine structure and pharmaceutical composition comprising the compound The present invention relates to a bicyclic pyrimidine compound of the following formula (I) or a salt thereof. wherein R1 is lower alkyl, cyclic lower alkyl. etc.; R2 is H, lower alkyl, lower alkenyl, etc.; R3 is H, lower alkyl, lower alkenyl, etc.; X is O, S or -N(R4)-; R4 is H or lower alkyl; or R2 and R4 may combine each other to form cyclic amino; Y is amido, keto, sulfonyl, etc.; R5 is H or lower alkyl; Z is O or S; m and n are 1 or 2. Said compound (I) or a salt thereof have MGAT inhibitory activity, and are useful as an agent for treatment or prophylaxis of adiposity, metabolic syndromes, hyperlipidemia, hyper neutral lipemia, hyper VLDL-mia, hyper fatty acidemia, diabetes mellitus, arteriosclerosis.
EP2368555A1 Compositions and methods of use of phorbolesters Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of cytopathic diseases. Cytopathic diseases may be caused by a variety means such as viral infections like HIV and AIDS, or the development of neoplasms in a mammalian subject. The methods and compositions of the invention are effective for inhibiting de novo HIV infection, upregulating viral expression from latent provirus, inhibiting HIV-induced cytopathic effects, down regulating the HIV receptor, increasing Thl cytokine expression, decreasing Th2 cytokine expression, increasing ERK phosphorylation, inducing apoptosis in malignant cells, inducing remission, maintaining remission, as chemotherapeutic agents, as well as for decreasing symptoms of cytopathic diseases and opportunistic infections that may accompany such diseasesl. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent such as those used in HAART protocols, therapeutic agents used to treat opportunistic infections due to HIV, or chemotherapeutic agents to yield more effective treatment tools against cytopathic diseases in mammalian subjects.
EP1514541A1 Use of bicyclic amino acids for preventing and treating visceral pain and gastrointestinal disorders The present invention relates to the use of compounds of formula I-III:
EP1845997A2 Apoptosis-inducing antineoplastic silver (i) coordination complexes The present invention describes chemotherapeutic compositions, a method for making the same, and methods for inducing apoptosis in tumor cells and/or inhibiting tumors. The compositions are metal coordination complexes of a cytotoxic metal, such as silver(I) and a chiral α-organic acid, such as tartaric acid, in a pharmaceutical carrier.
WO2014013727A1 Immunemodulating agent Provided is an immunomodulating agent for modulating abnormal immunity, particularly an excess immune response. The present inventors have made extensive studies. As a result, it is found that a mangosteen peel extract produced by extracting a mangosteen peel with a polar solvent has a function of modulating immunity, and the mangosteen peel extract is provided as an immunomodulating agent.
CN103751141A Rupatadine fumarate tablets and preparation method thereof The invention discloses rupatadine fumarate tablets and a preparation method thereof, belonging to the technical field of medicine. The tablets are prepared by making granules from rupatadine fumarate as active ingredient, and pharmaceutical adjuvants including a filler, a binder and a disintegrant, adding a lubricant, and making into tablets. Through the screening of the type and use amount of the filler, disintegrant, binder and lubricant and the use of specific sieving mesh to sieve raw materials during a preparation process, the prepared tablets have stable properties, good content uniformity, good dissolution, small tablet weight difference and high stability, so as to ensure in vivo bioavailability and clinical curative effect.
WO2008111271A1 Oral composition for nourishing the hair and stimulating hair growth An oral composition having effects of nourishing the hair and stimulating hair growth. A food material comprising cultivated kombu (edible kelp belonging to the genus Laminaria) rhizoid is used in an oral composition for nourishing the hair and stimulating hair growth. This oral composition may be used in the form of a nutritional supplement. Alternatively, it may be added to foods or drinks commonly used.
CN102188400A Sustained-release azithromycin matrix tablets and preparation method thereof The invention provides sustained-release azithromycin matrix tablets, which contain the following components in part by weight: 100 parts of azithromycin, 50 to 100 parts of hydroxypropyl methylcellulose, 10 to 20 parts of ethyl cellulose, 10 to 20 parts of No. II acrylic resin, and a proper amount of pharmaceutically acceptable filler. The sustained-release azithromycin matrix tablets can prolong the half-life period of medicaments, and are particularly suitable for single-time large-dose administration.
EP2199283A1 Prophylactic and/or therapeutic agent for anemia, comprising tetrahydroquinoline compound as active ingredient Disclosed is a low-molecular-weight compound having an EPO production-promoting activity and/or a hemoglobin expression-enhancing activity. Specifically disclosed is an EPO production promoter and/or a hemoglobin expression enhancer comprising a 1-acyl-4-(phenoxy, benzyloxy or phenylamino)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by the general formula (1); [wherein R1, R2, R2', R3 and R3' independently represent a hydrogen atom, a C1-6 alkyl group, or the like; R4, R5, R6, R7, R8, R9 and R10 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or the like; A represents N-R11 or an oxygen atom; R11 represents a hydrogen atom, a C1-6 alkyl group, or the like; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.
US6977246 Certain dinucleotides and their use as modulators of mucociliary clearance and ciliary beat frequency The present invention relates to certain novel dinucleotides and formulations thereof which are highly selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. They are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, PCD, cystic fibrosis, as well as prevention of pneumonia due to immobility. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis, otitis media and nasolacrimal duct obstruction. They are also useful for treatment of dry eye disease and retinal detachment as well as facilitating sputum induction and expectoration.
US20080118580 plant extracts contains terpenes, plant extracts, and cinnamic acid, use as fungicide for textile treatment; fucoidine, anethol, geraniol, farnesol or farnesol acid; low concentrations and reduce side-effects The invention relates to the use of substances that influence fungal dimorphism for reducing the adhesion of fungi to surfaces. The invention also relates to washing and/or cleaning agents, textile treating agents and cleaning agents for mouth, teeth or dentures and to the use of said substances in said agents. The inventive substances are selected from propolis extracts, plant extracts, cinnamic acid and the derivatives thereof, monoterpenes, sesquiterpenes and diterpenes and the derivatives thereof, especially fucoidine, anethol, geraniol, farnesol or farnesol acid.
US20130123255 Combination of a pi3k inhibitor and a mek inhibitor The invention relates to a method for the treatment of a patient with a proliferative disease including solid tumors, hematological malignancies and hyperplasia comprising administering a therapeutic combination to said patient wherein the therapeutic combination comprises a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of a compound of formula (II) or a pharmaceutically acceptable salt thereof.
WO2011001913A1 Ppar ligand Disclosed is a ligand for peroxisome proliferator-activated receptor (PPAR) which originates in a safe food material. Specifically disclosed is a PPAR ligand which comprises, as the active ingredient, a Luffa acutangula L. extract or a novel compound contained in the Luffa acutangula L. extract. This PPAR ligand is efficacious in preventing and/or ameliorating obesity and obesity-related disorders such as insulin resistance, hyperlipemia, hypertension, diabetes, etc.
WO2010045381A2 Antimicrobial agents that target bacterial vkor Aspects of the invention relate to a method for inhibiting the growth of a microbe that expresses bacterial vitamin K epoxide reductase (bVKOR). The method involves contacting the bacterial cell with an effective amount of an agent that inhibits bVKOR. Agents include a drug, ligand or portion thereof, protein, polypeptide, small organic molecule, antisense nucleic acid, RNAi, or antibody. Examples of useful agents are a phenylpropanoid, a modified phenylpropanoid, a coumarin or modified coumarin. A particularly useful agents is warfarin or a variant thereof or ferulenol or a variant thereof. The microbe is any microbe carrying a bVKOR gene, such as Mycobacterium tuberculosis.
EP2425832A1 Tormentic acid for the treatment of skin disorders Provided is a pharmaceutical composition for at least one selected from the group consisting of inhibiting the activity of matrix metalloproteinase (MMP), inhibiting the expression of matrix metalloproteinase, inhibiting the phosphorylation of mitogen-activated protein kinase (MAPK), and promoting the expression of collagen, comprising an effective amount of an active component selected from a group consisting of a compound of formula (I), a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable ester of the compound, and combinations thereof:
CN100998585A Injection containing meclofenoxate hydrochloride and its preparing method An injection of meclofenoxate hydrochloride and its preparing process which features use of non-water solvent chosen from alcohol, propanediol, glycerin, polyethanediol-300 and polyethanediol-400, and use of filter sterilizing method or wet-heat sterilizing method for high stability are disclosed.
US20100222394 Method for producing pyrazol-3-yl-benzamide derivative The present invention provides a more efficient industrial method for producing a pyrazol-3-yl-benzamide derivative expressed by a formula useful as medicine: wherein R2, R3 and R4 each independently represent a lower alkyl group.
US20120190705 Methods of inhibiting choroidal neovascularization The present invention relates to compositions and methods for inhibiting unwanted angiogenesis, particularly those of ocular tissues. The treatment, inhibition, and/or prevention of choroidal neovasculature (CNV) is provided, along with an animal model for CNV and imaging techniques that permit the screening of potential agents as anti-angiogenesis and anti-CNV agents.
US20090017131 Disinfectant cleaning composition and method Various embodiments of disinfectant cleaning compositions and the method of using them are provided. In one embodiment of the present invention, the disinfectant cleaning composition comprises, by weight, from about 0.5% to about 6% hydrogen peroxide and from about 0.5% to about 20% aloe vera and/or active thereof, and from about 99% to about 74% solvent. In another embodiment, the disinfectant cleaning composition can also include a fragrance.
WO2010125472A1 Use of collinsella aerofaciens for reducing bloating The invention relates to compositions comprising Collinsella aerofaciens for use for reducing bloating, in particular in subjects suffering from irritable bowel syndrome.
US7713972 Imidazotriazinone derivatives as PDE 7 (phosphodiesterase 7) inhibitors The present invention provides the compounds inhibiting PDE 7 selectively, and therefore, enhances cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is imidazotriazinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl group, R2 is methyl group; R3 is a hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; substituted or unsubstituted C1-C6 alkyl group; substituted or unsubstituted C2-C6 alkenyl group; saturated or unsaturated heterocycloalkyl group which is substituted or unsubstituted; a group: —NR5R6, —C(O)R7, —SO2R7, —OR8, —NR8COR7, —NR8S02R7; A is CR4; and B is CH.
CN103130725A Novel crystal form of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl (methylsulfonyl) amino] pyrimidin-5-yl] (3R, 5S)-3, 5-dihydroxy-heptyl-6-olefine acid and compound thereof The invention relates to a novel crystal form of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl (methylsulfonyl) amino] pyrimidin-5-yl] (3R, 5S)-3, 5-dihydroxy-heptyl-6-olefine acid and a preparation method for a compound thereof, in particular to a novel salification compound of rosuvastatin, specifically rosuvastatin magnesium and a crystal form thereof, and a preparation method and formulation and technology for an agent of acting medicine active ingredients of the compound. In animal experiments, the rosuvastatin magnesium in the crystal form has higher biological activity than rosuvastatin calcium and has good development prospects.
US20110135574 Methods of treating kidney disease It has been discovered that TRPC5 activity abolishes actin stress fibers and diminishes focal adhesion formation, rendering a motile, migratory podocyte phenotype. This invention relates generally to methods of reducing expression or activity of TRPC5 to treat, or reduce risk of developing, kidney disease, e.g., proteinuria, in a subject.
WO2014143607A1 Pyrrolopyridazines as potassium ion channel inhibitors A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
WO2007098681A1 Use of a monoterpene in manufacturing medicaments for treating diabetes mellitus Use of a monoterpene d-limonene in the field of pharmacy, particularly use of d-limonene in manufacturing medicaments for treating diabetes mellitus. In the experiments using the rat models of type I and type II diabetes mellitus, it shows that d-limonene can decrease the fasting blood glucose level markedly, thereby it proves that d-limonene is a potent medicament for treating type I and type II diabetes mellitus. Several clinical tests have proven that d-limonene can decrease postprandial blood glucose of type II diabetes mellitus patient markedly and stably. The toxicity of d-limonene is low and thereby it shows d-limonene is highly safe when it is administered orally. The source of d-limonene is rich, its price is cheap, and the extraction method is easy. D-limonene is extracted from the peel essential oils of citrus such as lemon and orange by the methods of cold compression or fractional distillation. This novel medicament is liquid and oily compound extracted from natural plants, other than the chemical synthesis compounds such as biguanides, sulfonylureas or glucosidase inhibitors.
US20080279775 Benztropinamine Analogs as Dopamine Uptake Inhibitors Disclosed are benztropinamine analogs having the formula I (I) in which E is NR1, S, or CH2; B is NR4, O, or CH2; m=1 to 5; n=1 to 3; Ar is a C5-C20 monocyclic aryl group or a C10-C20 bicyclic aryl group or a heteroaryl group having 2 to 6 carbon atoms and one or more heteroatoms selected from the group consisting of N, O, S, and any combination thereof; and bond “a” can be of α, β, or α/β configuration, wherein R1 to R5 are as described in the specification; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions and use thereof, e.g., in treating mental disorders.
CN1713911B Medicament component of berberine for the use of prevention and treatment of psycological dependence on and analgesic tolerance to morphine Disclosed is a pharmaceutical composition for preventing and treating addiction to morphine or preventing and inhibiting the development of tolerance to the analgesic effects of morphine, containing berberine as an effective ingredient, wherein the berberine has an inhibitory effect versus psychological dependence on abused drugs such as morphine and the increase of spontaneous locomotor activityupon administration of the drugs, The pharmaceutical composition and a Coptis japonica plant extract of the present invention, which contain berberine, are highly effective in inhibiting the aforementioned symptoms of morphine addiction, and are thus useful for prevention and treatment of addiction to abused drugs such as morphine. In addition, the pharmaceutical composition additionally containing a pharmaceutical acceptable carrier can be applied to prevent and inhibit morphine tolerance caused by repeated administration of morphine, while not affecting the analgesic effects of morphine upona single administration.
CN101768139A Piperazine derivative and preparation method and application thereof The invention provides piperazine derivatives and medicinal salts thereof. TAK-220 and Maraviroc are used as leading compounds, piperidine rings in the structure of the TAK-220 and Maraviroc are replaced by piperazine rings on the basis of the principle of isosteric replacement, and branch chains similar to Maraviroc are introduced to obtain piperazine derivatives. According to the preliminary pharmacological activity screening, the compounds have antagonism CCR5 activity and can be used for preparing CCR5-mediated drugs for curing diseases such as HIV infections, autoimmune diseases and the like. The invention has the following structural general formula as shown in the accompanying drawing.
US20130022610 Methods of decreasing glycosylated hemoglobin in patients with dyslipidemia Methods for treating abnormal glycosylated hemoglobin (HbA1c) levels in a patient in need thereof, wherein the provided methods comprise administering to a patient in need a therapeutically effective amount of an Interleukin-1β modulator. Also, the invention provides compositions comprising at least one lipid modifying agent and an IL-1β modulator.
CN102370628A Tetra-acetylated puerarin self-microemulsified sustained-release double-layer tablet and preparation method thereof The invention discloses a tetra-acetylated puerarin self-microemulsified sustained-release double-layer tablet and a preparation method thereof. The tetra-acetylated puerarin self-microemulsified sustained-release double-layer tablet comprises an outer quick-release layer and an inner sustained-release layer, wherein the quick-release layer mainly comprises tetra-acetylated puerarin, a self-microemulsion system, micro silica gel powder, microcrystalline cellulose, crosslinked polyvinylpyrrolidone and 5-20% starch slurry; the sustained-release layer mainly comprises tetra-acetylated puerarin, the self-microemulsion system, micro silica gel powder, hydroxypropyl methyl cellulose, polyoxyethylene, partially pregelatinized starch, iron oxide yellow and about 95% ethanol; the self-microemulsion system is composed of propylene glycol laurate, Tween 80 and ethylene glycol monomethyl ether; and the weight ratio of the quick-release layer to the sustained-release layer is 1: (3-5). The tetraacetyl puerarin self-microemulsified sustained-release double-layer tablet is a product combining a self-microemulsion technique and a sustained and controlled release technique, thus the bioavailability can be improved and the blood concentration can be more stable.
US20110212925 Novel compounds as receptor modulators with therapeutic utility The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
WO2012001308A9 Method for synthesizing ergoline alkaloids from indolic bicyclic compounds by double cyclization, resulting materials, and intermediate materials The present invention relates to a method for preparing structural analogues of tetracyclic, pentacyclic, and polycyclic ergoline alkaloids, in four steps, from an indole-3-carboxaldehyde, wherein the method includes the following two key steps: a step of coupling an N-protected 4-iodized 3-fluorinated indolic analogue with an unsaturated dipolarophilic function promoter, in particular an organostannic compound, thus leading to 3-formyl-4-alkenylindole or 3-formyl-4-alkynylindole. Said intermediates comprise an aldehyde function, which is converted into azomethine ylide, as well as a dipolarophilic unsaturated function that enables the dipolar reaction [3+2] of the second key step. The cyclization reaction, i.e. cycloaddition, is performed with an α-amino-functionalized compound, for example an α-aminoester compound, and, after condensation and cycloaddition, results in anticipated tetracyclic, pentacyclic, and polycyclic indoles.
CN102772399A Application of gambogic acid serving as protein kinase agonist activated by 5'-ampicillin (AMP) The invention discloses an application of gambogic acid serving as a protein kinase agonist activated by 5'-ampicillin (AMP), and relates to an anthranone type compound gambogic acid. The protein kinase agonist activated by the 5'-AMP is a novel anthranone type AMPK agonist and can be used for treating various diseases caused by metabolic disorder. The gambogic acid is (z-methyl-3-pentenyl)-;1,5-dimethylene-1,3-11-three-hydrogen-furan and (3,4-g)pyran and (3,2-b)anthranone-1-crotonic acid and is golden yellow crystals; the optical activity is 685 degrees (methanol); and the gambogic acid is dissolved in water difficultly and can be well dissolved in an organic solvent such as the methanol. The gambogic acid has relatively high bonding effect with the AMPK; the dissociation constant is 10<-6>M; and the gambogic acid can activate AMPK and protein acetyl coenzyme A carboxylase at the downstream of the AMPK, so that the gambogic acid can serve as the protein kinase agonist activated by 5'-AMP.
CN101347621A Medicament composition for treating respiratory disease The invention provides a pharmaceutical composition for the treatment of respiratory diseases, in particular asthma, rhinitis or COPD and especially asthma. Particularly, the composition contains glucocorticoid and leukotriene antagonist, especially Ciclesonide, Montelukast and salts usable for treatment. The pharmaceutical composition can be prepared to compound respirable powder and aerosol, irrespirable powder and aerosol and pressurized spray.
CN101791300A Acipimox push-pull osmotic pump controlled release tablet and preparation method thereof The invention belongs to the technical field of medicinal preparations, which discloses an acipimox push-pull osmotic pump controlled-release tablet and a preparation method thereof. The acipimox push-pull osmotic pump controlled-release tablet comprises a label and a controlled-release coating membrane which is coated outside the label and has medicine-release holes, wherein a medicine layer comprises the following components: 250mg of acipimox, 100-300mg of supensoid agent, 10-80mg of permeation pressure active substance, 2-7mg of lubricant and proper bonding agents; a boosting layer comprises the following components: 50-150mg of swelling agent and 5-50mg of permeation pressure active substance; a semipermeable coating membrane comprises the following components: 10-20g of semipermeable high polymer material, 2-6g of water-solubility pore-foaming agent and proper organic solvents; the weight of the coating membrane is 6-12 percent of the weight of the label, and 1-2 medicine-release holes are prepared on a medicine-content layer of a coating tablet by a laser or power drill. By regulating the label and a coating membrane prescription, the acipimox push-pull osmotic pump controlled release tablet can effectively regulate the constant release rate of medicines, thereby obtaining balanced blood concentration, reducing medicine-taking times, increasing the compliance of patients and achieving good lipid-regulating effect.
CN102006853A Topical composition for external use and process for producing the same A topical composition for external use comprising: a ceramide analogue-containing particle having a particle diameter of 0.001 [mu]m to 0.2 [mu]m; and a water-soluble polymer. It is preferable that, further, an oil component different from the ceramide analogue is contained in an amount of 20 parts by mass or less relative to 1 part by mass of the ceramide analogue-containing particle, and the ceramide analogue-containing particle is present in the oil component.
WO2009127612A1 Novel pyrazole derivatives The present invention relates tonovel pyrazolederivatives of Formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is C1-C4 alkyl or C1-C haloalkyl; R2 is an optionally substituted aryl or heteroaryl; R3 is halogen; R4 is hydrogen, halogen, C1-C4 alkyl, C1-C4 haloalkyl, cyano or OR6; R5 is hydrogen, halogen, C1-C4 alkyl, C1-C4 haloalkyl, cyano or OR6; R6 is hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C3-C10 alkylcycloalkyl, C1-C6 haloalkyl, C2-C6 alkenyl, C2-C haloalkenyl, C3-C7 cycloalkenyl, C2-C6 alkynyl, C2-C6 haloalkynyl, C2-C6 alkyloxyalkyl; R7 is halogen or OR6; X is N or C-R4; or an agrochemically usablesalt form thereof.
EP2549989A1 Compounds targeting the vegf and/or hif pathway such as sorafenib or vatalanib for use in the treatment of otitis media The present invention provides a compound which targets the VEGF and/or HIF pathways for use in the treatment and/or prevention of otitis media in a subject. The invention also provides a pharmaceutical composition comprising such a compound and a method for treating and/or preventing otitis media in a subject which comprises the step of administering such a compound or pharmaceutical composition to the subject.
US20080167324 Thiazolymethyl and Oxazolylmethyl Heteroaryl Derivatives Compounds of Formula I are provided, as are methods for their preparation. The variables in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agents(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
CN102357247A Therapeutic methods and delivery systems utilizing sex steroid precursors Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to either of the foregoing, are utilized for the treatment of vaginal atrophy, hypogonadism, diminished libido, loss of collagen or connective tissues in the skin, and, in combination with an estrogen and/or progestin, for the treatment of menopause. The precursors may be formulated for percutaneous or transmucosal administration. Gels, solutions, lotions, creams, ointments and transdermal patches for the administration of these precursors are provided, as are certain pharmaceutical compositions and kits which can be used for the prevention and treatment of a wide variety of conditions related to decreased secretion of sex steroid precursors by the adrenals.
US7402600 Nitroderivatives of cardiovascular agents Compounds or their salts having general formulas (I) and (II) wherein: s=is an integer equal to 1 or 2, preferably s=2; b0=0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.
CN102716496A Clathrate compound of scutellarin and alkaline cyclodextrin and preparation method thereof The invention discloses a clathrate compound of ionic scutellarin and alkaline cyclodextrin and a preparation method thereof. The alkaline cyclodextrin is amido substituted cyclodextrin, amido of the alkaline cyclodextrin is substituted, a cyclodextrin cavity and a scutellarin molecule have clathration, an alkaline environment is formed in aqueous solution, and ionic interaction is formed by the alkaline environment and hydroxyl or hydroxyl on the ionic medicament scutellarin, so that the scutellarin forms solution in water in a wide concentration range, and medicament scutellarin liquid preparation is conveniently formed. The clathrate compound is high in stability, good in safety, good in dissolubility, high in bioavailability, simple in preparation method, easy to operate, low in cost, soft in reaction condition, and applicable to industrial production.
WO2007119815A1 Toll-like receptor 9 agonists Toll-like receptor 9 (TLR9) agonists containing as the active ingredient compounds represented by the general formula (I) or pharmacologically acceptable salts thereof: wherein a is 0 or 1; n is an integer of 0 to 2; m is an integer of 0 to 5; X1 and X2 are each independently hydrogen or hydroxy; Y is oxygen or sulfur; -Q1- is –O- or the like; -Q2- is –O- or the like; -Z- is –O- or the like; R1, R3 and R4 are each independently hydroxy or the like; R2 and R5 are each independently hydrogen, hydroxy or the like; and A is 6-aminopurin-9-yl or the like.
CN101716323B Anti-fatigue medicine composition and preparation method thereof The invention belongs to the field of medicine, which in particular relates to an anti-fatigue medicine composition. The invention solves the technical question of providing a fire-new medicine composition used for resisting fatigue. The medicine composition is prepared from the following raw material medicines according to proportioning by weight: 5-15 parts of ginseng, 10-15 parts of rhizoma zedoariae, 5-15 parts of medlar, 5-15 parts of astragalus root, 1-10 parts of tuber fleeceflower and 5-15 parts of rhizoma ligustici wallichii.Pharmacological experiments prove that the medicine composition has an anti-fatigue function after being orally taken and externally applied.The medicine composition is prepared into an externally-applied preparation matched with massage and applied to clinical treatment, can alleviate fatigue syndrome caused by excess brainwork, excess physical labour or the long-term tension of the spirit, such as the symptoms of energy deficiency, fatigue, wimpization,distractibility, chest distress, palpitation, insomnia, amnesia and the like, and has obvious curative effect.
US20080009476 Treating conjunctivitis by topically administering an epinastine solution to the conjunctiva Treating allergic conjunctivitis by administered aqueous solutions containing epinastine, optionally in the form of its racemate or its enantiomers and optionally, in the form of the pharmacologically acceptable acid addition salts thereof, to the conjunctiva.
EP1968561B1 Treatment of diabetic nephropathy Disclosed herein are methods, compounds and compositions for preventing or treating a renal disorder or chronic kidney diseases, including nephropathies such as diabetic nephropathy. The invention generally includes administering to a subject 1,3-propanedisulfonic acid or a pharmaceutically acceptable salt thereof, e.g., 1,3- propanedisulfonic acid sodium salt. The invention also relates to methods, compounds and compositions for the prevention and/or treatment of for preventing or treating a renal disorder complication. The invention further relates to methods, compounds and compositions for the prevention and/or treatment of dyslipidemia, and more particularly for reducing levels of harmful serum lipid levels, especially cholesterol and triglycerides in diabetic patients.
WO2007055928A1 5-membered ring metanicotine analogs E-metanicotine-type compounds that include a five-membered heteroaryl ring linked to an olefinic linker, such as a 4-penten-2-yl linker, which is linked to a terminal amine group, are disclosed. Patients susceptible to or suffering from conditions and disorders, can be treated by administering the compounds, pharmaceutical salts of the compounds, or pharmaceutical compositions including the compounds or their salts, to a patient in need thereof.
CN102846993A Externally-used plaster for treating infantile febrile convulsion The invention discloses an externally-used plaster for treating infantile febrile convulsion. The externally-used plaster is characterized in that bulk pharmaceutical chemicals of the formula weight are grinded into powder, then wine with the alcoholic strength lower than 40 degrees is slowly dropped into the medicine powder to stir the medicine into paste while the wine is dropped. The bulk raw materials comprises by weight proportion: 0.5-2 parts of amber, 2 parts of pearl, 1 part of bezoar, 1 part of rhinoceros horn, 1 part of stiff silkworm, 1 part of periostracum cicada, 1 part of bulbus fritilariae, 1 part of pericarpium citri reticulatae, 0.5-1 part of bryozoatum, 2 parts of fructus piperis alba, 0.5-2 parts of fructus evodiae or 0.5-2 parts of concretio silicea bambusae and/or 0.5-2 parts of arisaema cum bile, 2 parts of sticky rice, 0.5-2 parts of jasmine or 0.5-2 parts of rheum officinale and 0.5-2 parts of uncaria rhynchophylla or 0.5-2 parts of gastrodia elata. The externally-used plaster for treating infantile febrile convulsion is good in effect of preventing and treating infantile convulsion, free of side and toxic effects, wide in medicine source and moderate in cost, has the effect of wind dispelling, resuscitation inducing, dizziness relieving, convulsion relieving, tranquilizing and excitement allaying, phlegm cleansing and spasmolysis, and is suitable for children patients, and the cure rate is as high as 95%.
WO2010015523A1 Cyclohexyloxy-substituted heterocyclics, medicines containing these compounds and method for the production thereof The present invention relates to cyclohexylol-substituted heterocyclics of the general formula (I), to tautomers thereof, to stereoisomers thereof, to mixtures thereof and to salts thereof, in particular physiologically compatible salts thereof containing inorganic or organic acids and bases and having valuable pharmacological properties, in particular an inhibiting effect on the signal transduction mediated by tyrosine kinases, to the use thereof in the treatment of illnesses, in particular tumor diseases and benign prostate hyperplasia (BPH), diseases of the lungs and respiratory tracts, and to the production thereof.
CN103099900A Tendon relaxing, meridian activating and pain stopping powder and preparation method thereof The invention discloses tendon relaxing, meridian activating and pain stopping powder. The tendon relaxing, meridian activating and pain stopping powder comprises the following raw materials in parts by weight: 20-30 parts of semen strychni, 20-30 parts of ephedra, 10-20 parts of angelica root, 10-15 parts of rough haired holly root, 10-20 parts of frankincense, 15-20 parts of myrrh, 20-30 parts of forging native copper, 20-30 parts of safflower, 10-20 parts of zaocys dhumnade, 20-30 parts of szechuan lovage rhizome, 30-35 parts of lycopodium clavatum, 15-20 parts of rhizoma corydalis, 20-30 parts of pseudo-ginseng, 20-30 parts of Indian damnacanthus herb, 10-15 parts of monkshood and 20-30 parts of erythrinae bark. The pain stopping powder disclosed by the invention is mainly used for treating lumbar disc herniation, cervical spondylosis, scapulohumeral periarthritis, hyperostosis, arthritis, rheumatism pain or numbness, bone-setting bruising pain and numbness of muscles and bones, as the medicinal materials have the effects of activating blood, dissolving stasis, getting through blood vessel, expelling wind, removing cold and promoting normal and unobstructed blood circulation and follow the principle that no ache is caused while breathe is smooth, a factor with certain stimulation is utilized, local blood vessels are expanded, blood circulation is promoted, and nutrition of tissues at the periphery is improved, so that the effects of promoting qi to activate blood and diminishing inflammation to stop swelling are achieved.
CN1600300A Compound external remedy for treating psoriasis An externally-applied compound medicine in the form of ointment, cream, lotion, liniment or aerosol for treating skin tinea is prepared from butenafine hydrochloride, other antifungal medicines (salicylic acid, spirofulvin, amorolfine, etc), and assistant.
EP1299430B1 Process for preparing benzoxazin-4-one polymer conjugates The present invention relates to a process for forming polymer conjugates which are useful as enzyme inhibitors. The process of the present invention comprises the steps of:a) reacting a polymer or copolymer having the formula (1) wherein R is a hydrocarbyl moiety, a polyalkyleneoxy moiety, or a heteroatom comprising hydrocarbyl moiety, said polymer or copolymer having a molecular weight of from about 500 daltons, with phosgene to form a chloroformate having the formula (2); b) combining a substituted or unsubstituted anthranilic acid having the formula (3) wherein each R1 unit is an enzyme interaction attenuating unit; and a base catalyst wherein said base catalyst is a supported base catalyst, to form a substrate reactive admixture; and c) adding to said chloroformate formed in step (a) said substrate reactive admixture formed in step (b) to form a benzoxazin-4-one conjugate having the formula (4).
EP1071764B1 Antisense oligonucleotides for the inhibition of integrin alphav-subunit expression The present invention relates to an antisense oligonucleotide or a derivative thereof which has a sequence that corresponds to a part of a nucleic acid which encodes an integrin αv subunit and which has the ability to induce apoptosis, the preparation and the use thereof.
US20130018028 Bi-(indole-2-aceto)-iron II (Ferrous Indole Acetate) Bi-(indole-2-aceto)-iron II, also named ferrous bis(indole acetate), or a pharmaceutically acceptable salt thereof, wherein: —Fe (Iron) is substituted by another transition metal capable of bonding to two molecules of indole acetate is synthesized for medicinal purposes including treatment of solid tumor cancers and other vascular proliferative disorders. This invention also extends to the substitution of the ligands by one or more of the structural analogues of indole acetetate disclosed in this application. In certain aspects, the compositions of the invention are capable of generating both a vascular targeting effect and tumor cell cytotoxicity (e.g. by oxidative stress) in order to achieve an enhanced anti-tumor response.
CN101214287A Medicament for treating otitis medis The present invention discloses a medicine for curing tympanitis, which is made from the following components with the weight portions: 1 to 3 portions of borneol, 4 to 6 portions of globeflower, 3 to 7 portions of forsythia fruit, 2 to 4 portions of creat and 3 to 5 portions of antibiotic. The present invention has the advantages of scientific prescription and mixed application of refreshing the mind, clearing away heat and alleviating pain by borneol; removing heat and toxic substance by globeflower; relieving swelling, resolving masses and cooling the blood by forsythia fruit and creat; and the western medicine antibiotic, thus producing quicker results. The present invention with abundant raw materials, low price, simple preparation and good curing effect has cure rate of ear internal pyorrhea, secretory otitis media, ear pain and other diseases up to more than 96 percent.
US20110165211 Carbon dioxide external preparation, and material for formation of carbon dioxide external preparation A material for formation of carbon dioxide external preparation of the present invention comprises a base agent and a reactant. The base agent comprises a polymeric three-dimensional network structure impregnated with a viscous material containing at least an acid and water, and is made to contact with the skin in use. The reactant contains at least a carbonate, and contacts with the aforementioned viscous material in use so as to generate carbon dioxide, the carbon dioxide dissolving in the viscous material substantially in a non-bubble state.
US8019557 Cavity induced allosteric modification of intermolecular interactions and methods of identifying compounds that effect the same Method of identifying compounds that modulate intermolecular interactions between a target protein and a modifier are disclosed. Pharmaceutical composition comprising compounds that inhibit intermolecular interactions between a target protein and a modifier are disclosed. Methods of treating individual suffering from inflammatory conditions, undesirable immune responses, immunological conditions and bacterial infections are disclosed.
EP1501847A2 11-deoxy azalide antibacterials Antibacterial compounds having formula (I) and formula (II), and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates used in the processes, compositions containing the compounds, and methods for prophylaxis or treatment of bacterial infections using the compounds are disclosed.
US20110166201 Mirnas as therapeutic targets in cancer MicroRNAs (miRNAs) are a class of non-coding small RNA molecules that regulate gene expression at the post-transcriptional level by interacting with 3′ untranslated regions (UTRs) of their target mRNAs. The invention relates to the application of miR-192 and miR-215. Both of these miRNAs impact cellular proliferation through the p53-miRNA circuit, and interact with dihydrofolate reductase (DHFR) and thymidylate synthase (TS). Particularly, upregulation of these miRNAs reduces cellular proliferation. The invention relates to this discovery. For example, inhibiting miR-192 and/or miR-215 sensitizes a neoplasm or a subject with a neoplasm to chemotherapeutic agents. Furthermore, measuring the levels of miR-192 and/or miR-215 provides one with information regarding whether the neoplasm or subject will respond to chemotherapeutic agents. Accordingly, the invention relates to composition and methods relating to the identification, characterization and modulation of the expression of miR-192 and miR-215.
EP2603213A2 Methods of treating obstructive lung diseases using bitter tastants Described herein are methods for enhancing airway dilation and/or relieving bronchoconstriction, e.g., to treat obstructive lung diseases such as asthma and COPD, by administering bitter tastants to subjects in need thereof. Also described herein are methods for identifying compounds that modulate function of bitter tastant receptors.
EP1513526B1 Phenylalkanoic acid and phenyloxyalkanoic acid derivatives as hppar activators The present invention provides a compound of formula (I):wherein:R1 and R2 are independently H or C1-3 alkyl;X represents a O or (CH2)n where n is 0, 1 or 2;R3and R4 independently represent H, C1-3 alkyl, -OCH3, -CF3, allyl, or halogen;X1 represents O, S, SO2, SO, or CH2;R5 and R6 independently represent hydrogen, C1-6 alkyl (including branched alkyl and optionally substituted by one or more halogens or C1-6alkoxy), or together with the carbon atom to which they are bonded form a 3-6 membered cycloalkyl ring;R7 represents a phenyl or a 6 membered heteroaryl group containing 1, 2 or 3 nitrogen atoms wherein the phenyl or heteroaryl group is substituted by 1, 2 or 3 moieties selected from the group consisting of halogen, C1-6 alkoxy, C1-6 alkyl, CF3, hydroxy, or phenyl (which may be optionally substituted by one or more C1-3 alkyl, -OC1-3 alkyl, CN, acetyl, hydroxy, halogen or CF3).
CN1997630A New disubstituted phenylpiperidines as modulators of dopamine neurotransmission The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho, meta-disubstituted phenyl)-1-alkypiperidines and piperazines, wherein R1, R2, R3 and Y are as defined.
US20080125460 inducible nitric oxide synthase inhibitors; acute or chronic inflammatory diseases of of peripheral organs and the central nervous system; 6-pyridinyl imidazo-[4,5-b]pyridine compounds; 2-[2-(4-Methoxypyridin-2-yl)ethyl]-6-(pyridin-4-yl)-3H-imidazo-[4,5-b]pyridine The compounds of Formula (I) in which R1, R2, Het1 and A have the meanings as given in the description are novel effective iNOS inhibitors.
CN102850363A Irinotecan hydrochloride compound and pharmaceutical composition thereof The invention belongs to the technical field of medicine, and particularly relates to an irinotecan hydrochloride compound and a pharmaceutical composition thereof. The irinotecan hydrochloride compound is a crystal; the molecular formula of the irinotecan hydrochloride compound is C33H38N4O6.HCl.3H2O; the powder X-ray diffraction process on the irinotecan hydrochloride compound determines that the X-ray diffraction spectrum represented by the 2 theta +/-0.2 degree diffraction angle has characteristic diffraction peaks at 10.3 degrees, 10.6 degrees, 14.9 degrees, 16.9 degrees, 17.9 degrees, 20.2 degrees, 20.8 degrees, 26.7 degrees, 29.8 degrees and 30.5 degrees. The invention also provides a preparation method of the irinotecan hydrochloride and a pharmaceutical composition containing theirinotecan hydrochloride compound. The irinotecan hydrochloride compound has high water solubility and high dissolution rate in water.
CN103690511A Method for preparing Ftorafur-loaded vesicle The invenetion discloses a method for preparing Ftorafur-loaded vesicle. The method comprises the following steps: performing one-step synthesis of mono[6-deoxy-N-butylamide]-beta-cyclodextrin by taking mono[6-p-toluenesulfonyl]-beta-cyclodextrin as a raw material, and performing self-assembly on the obtained compound and Ftorafur in an aqueous solution to form a novel Ftorafur vesicle preparation loaded with Ftorafur. According to the method, the technical problem that the Ftorafur is instable in water is effectively solved, the obtained vesicle aqueous solution has a slow release effect, an anti-cancer effect of the Ftorafur can be improved, and a novel preparation form is provided for clinical application of the Ftorafur.
US20120177750 Methods for treating pain using topical product formulations containing strontium Topical formulations containing aqueous-soluble divalent strontium cation in a suitable topical keratinized skin formulation vehicle, and methods of using these formulations to inhibit skin irritation in keratinized skin, are disclosed.
US6906196 Antiinflammatory agents, rheumatic disorders Provided are processes and chemical intermediates useful for preparing a compound of the formula I wherein X is selected from the group consisting of C1-C6 trihalomethyl; C1-C6 alkyl; and an optionally substituted or di-substituted phenyl group of formula II: Y and Z are independently selected from the group consisting of substituted and unsubstiotuted aryl
CN102180941B Derivatives of betulonic acid, method for preparing same and application thereof The invention relates to derivatives of betulonic acid, a method for preparing the same and application thereof. The method comprises the following steps of: under the protection of nitrogen gas and in the presence of alkali, condensing betulonic acid or hydrogenated betulonic acid serving as a raw material and ethyl formate, diethyl oxalate, diethyl carbonate or ethyl trifuoroacetate at the temperature of between 25 and 66 DEG C for 5 to 7 hours, performing cyclization on the obtained reaction product and hydrazine hydrochloride, oxammonium hydrochloride or phenyhydrazine hydrochloride at the temperature of 78 DEG C for 1 hour, and purifying the obtained product to obtain the derivatives of betulonic acid, wherein the yield is 63 to 85 percent. In the method, by importing heterocyclic rings at the positions of C2 and C3 of the natural product of betulonic acid, a series of derivatives with new structures are synthesized in high efficiency, the process is simple, and by the structuralmodification, the activity of the betulonic acid of inhibiting differentiation of osteoclasts is obviously enhanced.
US20120244096 Plant extract, compositions containing same, method of extraction and uses thereof An extract from leaves of mulberry is disclosed. The extract has an IC50 value sufficient to inhibit α-glucosidase I. The extract may comprise 5-40% (w/w) total imino sugars and 20-70% (w/w) total amino acids. The extract may reduce the production of melanin for the treatment of such ailments or diseases caused by pigmentation as freckle, chloasma, striae gravidarum, sensile plaque and melanoma. The extract may also control blood glucose level.
CN1771918A Granisetron cataplasm and its prepn The present invention relates to medicine technology, and is Granisetron cataplasm as 5-HT3 receptor agonist in new form. Granisetron is applied clinically in preventing and treating nausea, vomiting, etc caused by cytotoxicity treatment, and available Granisetron preparation forms have some demerits. The present invention prepares Granisetron into cataplasm with the hydrochloride or free alkali of Granisetron as main medicine component and some supplementary materials. The Granisetron cataplasm with transdermal administration has no first pass effect, reduced and constant systemic blood medicine concentration, less side effect, raised compliance and other advantages.
CA2148871C Method of preventing hyperproliferative vascular disease This invention provides a method of preventing hyperproliferative vascular disease in a mammal by administering an antiproliferative effective amount of rapamycin alone or in combination with mycophenolic acid.
WO2014109987A1 Mixed disulfide conjugates of thienopyridine compounds and uses thereof This invention is in the field of medicinal chemistry. In particular, the invention relates to mixed disulfide conjugates of thienopyridine compounds, and their use as therapeutics for the treatment, amelioration, and prevention of cardiovascular diseases.
EP2187897A1 Composition for preventing virus infection comprising poly-gamma-glutamic acid The present invention relates to a pharmaceutical composition for inhibiting or preventing viral infection, which comprises an effective dose of poly-gamma- glutamic acid(γ-PGA), and more particularly, to a pharmaceutical composition, a functional food, and a feedstuff additive capable of inhibiting viral infection and preventing viral diseases, which comprise poly-gamma-glutamic acid having an infection-inhibiting effect against viruses, such as an influenza virus, inducing respiratory infection or systemic infection, as an effective ingredient. The composition containing poly-gamma-glutamic acid as an effective ingredient according to the present invention, is effective for use as an animal feedstuff additive or a pharmaceutical agent for preventing influenza virus infection and various viral diseases as well as a pharmaceutical composition and a functional food to promote human health.
CN101987189A Detoxifying and channel dredging external application powder The invention relates to a Chinese patent medicament, in particular to external application powder for treating avascular necrosis femoral head, prolapse of lumbar intervertebral disc, hyperosteogeny, scapulohumeral periarthritis, ankylosing spondylitis, rheumatism and rheumatoid. Aiming at virtual and actual differentiation of symptoms and signs of patients, detoxifying and channel dredging capsules (another application) are orally taken and detoxifying and channel dredging powder is externally applied so as to directly reach a lesion site; starting from the integral concept, oral administration and external application are adopted for attacking from both inside and outside, relieving dizziness and stopping spasm, detoxifying and dissipating stagnation, expelling toxin and pus, eliminating putridity and engendering flesh, strengthening muscle and bone, supplementing insufficiency, strengthening healthy energy and recovering, so that qi and blood are smooth, essence and blood are vigorous, liver and kidney are nourished, bones are supplemented and strengthened, the blood is sufficient and the disease is healed.
CN102670507A Long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin and preparation method thereof The invention belongs to the technical field of medicine, and relates to a lyophilized powder for injection of a long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin and a preparation method thereof. The lyophilized powder for injection comprises 1%-30% of 7-ethyl-10-hydroxycamptothecin, 10%-90% of phosphatide, 0%-10% of octadecylamine, 0%-70% of a lyophilizing protective agent, 0%-50% of accessory G, 0.001%-50% of an antioxidant, 0%-30% of cholesterol, 0%-50% of thermal sensitive accessory H, and a balanced amount of a buffer solution. The long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin has improved water-solubility and stability, and has reduced toxicity.
CN101215281A Isoflavone sulfonate derivatives and synthetic method thereof An isoflavone sulfonates derivative and the synthesis process are characterized in that the chemical structural general formula is that R1 is OR3 and OCOR4, R2 is aromatic sulfonic acid ester group, and R3 and R4 is C1-C2 alkyl. The compound ester solubility of the invention is greatly improved compared with soybean aglycone.
CN1666751A Prescription for treating type 2 diabetes and its preparing method The invention discloses a prescription and its process method of health food or drug which can treat II diabetes. Available compositions and available parts of balsam, panax, and gynostemma pentaphylla as main materials are abstracted by modern bioengineering technique, and manufactured to be superior functional health food and drug with solid dispersion technique. And taking medicine sublingually can avoid stomach and intestine destroying available compositions, while promoting buccal mucosa capillary vessel directly absorbing available compositions, promoting salivation and deglutition, in result of reflexive enhancing actions of gastrointestinal tract and exudation of insulin, therefore have remarkable prevention and treatment on II diabetes.
CN103191062A Sulbenicillin sodium injection The invention provides sulbenicillin sodium injection. Freeze-dried sterile sulbenicillin sodium is used as a raw material and prepared into a product free of any solid auxiliary material or excipient by virtue of a sterile sub-packaging process; in terms of anhydrous substances, the content of the D(-)-sulbenicillin sodium is bigger than 99%, the content of the L(+)-sulbenicillin sodium is smaller than 0.5%, the content of the sulbenicillin sodium polymer is smaller than 0.3% and the content of moisture is smaller than 5%. Moreover, the sulbenicillin sodium injection has high product purity, strong anti-bacterial activity and good stability, so that medication safety of the human body can be ensured better.
WO2011079142A2 Purified pyrroloquinolinyl-pyrrolidine-2,5-dione compositions and methods for preparing and using same The present invention relates to a form 1 and form 2 polymorph of (-)-trans -3 -(5,6- dihydro-4H-pyrrolo [3,2,1-ij] quinolin-1-yl)-4-(1H-indol-3-yl) pyrrolidine-2,5-dione. The present invention also relates to (-)-trans-3-(5,6-dihydro-4H-pyrrolo [3,2,1-ij] quinolin-1-yl)-4- (1H-indol-3-yl) pyrrolidine-2, 5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (-)-trans-3-(5,6-dihydro-4H-pyrrolo [3,2,1-ij] quinolin-l-yl)-4-(lH-indol-3-yl) pyrrolidine-2, 5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (-)-trans- 3-(5,6-dihydro-4H-pyrrolo [3,2,1-ij] quinolin-l-yl)-4-(lH-indol-3-yl) pyrrolidine-2, 5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (-)-trans -3 -(5,6- dihydro-4H-pyrrolo [3,2,1-ij] quinolin-1-yl)-4-(1H-indol-3-yl) pyrrolidine-2,5-dione.
US20110152346 Use of Oligonucleotides with Modified Bases in Hybridization of Nucleic Acids The invention is concerned with the use of oligonucleotide analogs that contain specifically modified DNA bases to be used in hybridization of nucleic acids, polymerase chain reaction (PCR) and siRNA-mediated gene silencing (RNAi).
WO2009071483A1 1- (indaz0l-5-yl) -ureas as diacylglycerol acyltransferase inhibitors Provided herein are compounds of the Formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
EP1865948A1 Vitamin mixtures The present invention relates to a vitamin composition that strengthens and promotes retinal health, in particular in people being affected with AMD.
US20100256166 Novel Hydantoin Derivatives as Metalloproteinase Inhibitors The invention provides compounds of formula (I): wherein R1, R2, A, A1 and B are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds are useful as MMP inhibitors.
CN102309444A Novel docetaxel injection pharmaceutical composition and application thereof The invention discloses a novel docetaxel injection pharmaceutical composition, which comprises an A agent (micro-nano-docetaxel) and a B agent (a drug solvent). The docetaxel injection pharmaceutical composition disclosed by the invention is simple in production process and convenient to use. The docetaxel injection pharmaceutical composition can be stored at room temperature. The drug stability is prior to homemade and importation like products.
CN102670521A Esomeprazole magnesium enteric-coated pellet and preparation method thereof The invention belongs to the field of pharmacy and relates to a medicinal preparation taking esomeprazole magnesium as an active ingredient, in particular to an esomeprazole magnesium enteric-coated pellet and a preparation method thereof. According to the esomeprazole magnesium enteric-coated pellet, medicines can be rapidly released in intestinal tracts. The esomeprazole magnesium enteric-coated pellet comprises the following structural layers in sequence from inside to outside: a medicine-contained layer, an isolation layer and an enteric-coated layer.
WO2011141822A3 Methods for induction, predictive diagnosis, and treatment of affective behaviors by modulation of ppar and rxr receptors The present invention is directed to methods for modulating or detecting changes in peroxisome proliferator activated receptors (PPARs) and retinoid X receptors (RXR) to: 1) treat certain neuropsychiatric disorders, 2) identify susceptibility to such disorders in a clinical setting, and 3) screen novel pharmacological agents, including retinoids and retinoid derivatives for adverse psychiatric side-effects, and 4) generate certain neuropsychiatric disorders in preclinical conditions.
WO2007010910A1 1-benzyl-4-[(5, 6-dimethoxy-1-indanon)-2-yl]-methyl piperidine p-toluenesulfonate or crystal thereof 1-Benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine p-toluenesulfonate or a solvate thereof.
WO2009075557A1 Fluorobenzenamides having anti-convulsive activity The invention relates to novel methods for obtaining novel derivatives: DL-2-hidroxy-2-(3'-trifluoromethylphenyl) butyramide and DL-3-hidroxy-3-(3' or 4´- trifluoromethylphenyl) pentanamides, having general formula (I) wherein n is equal to zero and one and R1 and R2 are equal to H or CF3. The aforementioned compounds have anti-convulsive activity.
US20120122920 Libraries of n-substituted-n-phenylethylsulfonamides for drug discovery New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.
EP2332528A1 Substituted aromatic dicarbonic acid amides as medicaments Substituted aromatic dicarboxylic acid amide compounds (I) and their racemic mixtures, enantiomers, diastereomers, mixture of enantiomers, diastereoisomers or a single enantiomer or diastereoisomer and/or their salts, are new. Substituted aromatic dicarboxylic acid amide compounds of formula (I) and their racemic mixtures, enantiomers, diastereomers, mixture of enantiomers, diastereoisomers or a single enantiomer or diastereoisomer and/or their salts, are new. X : aryl group of formula (a1) or (a2); Y1 : O, S or (CH 2) m; m : 0-2; R1-R4 : H, F, Cl, Br, I, OR5, SR5, C(=O)OR5, CN, CF 3, NO 2, NR5R6, 1-10C-alkyl (optionally saturated, optionally branched, optionally substituted by one or more substituents), 3-10C-cycloalkyl or heterocyclyl (optionally bridged by 1-8C-alkyl, optionally saturated, optionally substituted by one or more substituents) or (hetero)aryl (optionally substituted by one or more substituents and optionally bridged by 1-8C-alkyl), where the alkyl chain is optionally branched, optionally saturated and optionally substituted by one or more substituents; and R5, R6 : H, 1-10C-alkyl (optionally saturated, optionally branched, optionally substituted by one or more substituents), 3-10C-cycloalkyl or heterocyclyl (optionally bridged by 1-8C-alkyl, optionally saturated, optionally substituted by one or more substituents) or (hetero)aryl (optionally substituted by one or more substituents and optionally bridged by 1-8C-alkyl), where the alkyl chain is optionally branched, optionally saturated and optionally substituted by one or more substituents, where the alkyl-, heterocyclyl- and cycloalkyl-substituents are F, Cl, Br, I, NO 2, CN, =O, CF 3, 1-8C-alkyl, (hetero)aryl, 3-10C-cycloalkyl, heterocyclyl, C(=O)OH, C(=O)O-1-8C-alkyl, C(=O)O-3-10C-cycloalkyl, C(=O)O-(hetero)aryl, C(=O)NH 2, C(=O)NH-1-8C-alkyl, C(=O)NH-3-10C-cycloalkyl, C(=O)NH-(hetero)aryl, C(=O)N(1-8C-alkyl) 2, C(=O)N(3-10C-cycloalkyl) 2, C(=O)N((hetero)aryl) 2, C(=O)N(1-8C-alkyl)(3-10C-cycloalkyl), C(=O)N(1-8C-alkyl)((hetero)aryl), C(=O)N(3-10C-cycloalkyl)((hetero)a ryl), C(=O)N(aryl)(heteroaryl), OH, OCF 3, O-1-8C-alkyl, O-3-10C-cycloalkyl, O-(hetero)aryl, O-C(=O)-1-8C-alkyl, O-C(=O)-3-10C-cycloalkyl, O-C(=O)-(hetero)aryl, SH, SCF 3, S-1-8C-alkyl, S-3-10C-cycloalkyl, S-(hetero)aryl, NH 2, NH-1-8C-alkyl, NH-3-10C-cycloalkyl, NH-(hetero)aryl, N(1-8C-alkyl) 2, N(3-10C-cycloalkyl) 2, N((hetero)aryl) 2, N(1-8C-alkyl)(3-10C-cycloal kyl), N(1-8C-alkyl)((hetero)aryl), N(3-10C-cycloalkyl)((hetero)aryl), N(aryl)(heteroaryl), NH-C(=O)-1-8C-alkyl, NH-C(=O)-3-10C-cycloalkyl and NH-C(=O)-(hetero)aryl, and the (hetero)aryl substituents are F, Cl, Br, I, NO 2, CN, CF 3, 1-8C-alkyl, (hetero)aryl, 3-10C-cycloalkyl, heterocyclyl, C(=O)OH, C(=O)O-1-8C-alkyl, C(=O)O-3-10C-cycloalkyl, C(=O)O-(hetero)aryl, C(=O)NH 2, C(=O)NH-1-8C-alkyl, C(=O)NH-3-10C-cycloalkyl, C(=O)NH-(hetero)aryl, C(=O)N(1-8C-alkyl) 2, C(=O)N(3-10C-cycloalkyl) 2, C(=O)N((hetero)aryl) 2, C(=O)N(1-8C-alkyl)(3-10C-cycloalkyl), C(=O)N(1-8C-alkyl)((hetero)ary l), C(=O)N(3-10C-cycloalkyl)((hetero)aryl), C(=O)N(aryl)(heteroaryl), OH, OCF 3, O-1-8C-alkyl, O-3-10C-cycloalkyl, O-(hetero)aryl, O-C(=O)-1-8C-alkyl, O-C(=O)-3-10C-cycloalkyl, O-C(=O)-(hetero)aryl, SH, SCF 3, S-1-8C-alkyl, S-3-10C-cycloalkyl, S-(hetero)aryl, NH 2, NH-1-8C-alkyl, NH-3-10C-cycloalkyl, NH-(hetero)aryl, N(1-8C-alkyl) 2, N(3-10C-cycloalkyl) 2, N((hetero)aryl) 2, N(1-8C-alkyl)(3-10C-cycloal kyl), N(1-8C-alkyl)((hetero)aryl), N(3-10C-cycloalkyl)((hetero)aryl), N(aryl)(heteroaryl), NH-C(=O)-1-8C-alkyl, NH-C(=O)-3-10C-cycloalkyl or NH-C(=O)-(hetero)aryl. [Image] [Image] - ACTIVITY : Analgesic; Antimigraine; Neuroprotective; Nootropic; Antiparkinsonian; Anticonvulsant; Eating-Disorders-Gen.; Anabolic; Anorectic; Ophthalmological; Neuroleptic; Antidiabetic; Antidepressant; Anesthetic; Antiemetic; Antiaddictive; Respiratory-Gen.; Laxative. - MECHANISM OF ACTION : Vesicular glutamate transporter 1 modulator; Vesicular glutamate transporter 2 modulator. The ability of (I) to inhibit vesicular glutamate transporter 1 was tested in rats. The results showed that 2-(3-(2-carboxy-5-nitrophenylcarbamoyl)benzamido)-4-nitrobenzoic acid exhibited an inhibitory activity of 92%.
WO2002050028A8 Substituted benzoindoles as spla2 inhibitors A novel class of benz[f]indole compounds see structure (I) is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shock.
CN103467359A Cinnamon amides histone deacetylase inhibitor with benzpyrole and preparation method and application of same The invention relates to cinnamon amides histone deacetylase inhibitor with benzpyrole and a preparation method and application of the innamon amides histone deacetylase inhibitor, and further relates to pharmaceutical compositions of compounds with the general formula (I) structures and pharmaceutical usage of the pharmaceutical compositions of compounds with the general formula (I) structures. The compound has good activity in vivo and in vitro and suitable for diseases with abnormal histone deacetylase activity, such as cancer.
US8709385 Poloxamer foamable pharmaceutical compositions with active agents and/or therapeutic cells and uses Pharmaceutical or cosmetic compositions and methods for their use are provided comprising water and a surfactant polymer system comprising a Poloxamer at a concentration of about 0.1% to about 15% by weight; wherein when the Poloxamer is between about 0.1% to about 5% Poloxamer. The composition can further comprise a supporting agent comprising a non-ionic surface active agent or a supporting agent comprising a non surfactant polymer or polysaccharide and an active agent, where the Poloxamer is capable of fixing the composition on delivery to a body surface. There are further provided therapeutic cell compositions and their uses.
EP2779842A1 Composition for protection against cell-damaging effects The present invention relates to a composition consisting of Vitamin C, L-glutamine, L-cystine or L-cysteine, riboflavin, succinic acid, fumaric acid, coenzyme Q10, and niacin. The present invention relates further to the use of the composition for minimizing the cell-damaging effect of radicals and harmful forms of oxygen, in particular of oxygen radicals or reactive oxygen species. The present invention relates to a composition comprising Vitamin C, L-glutamine, L-cystine or L-cysteine, riboflavin, succinic acid, fumaric acid, coenzyme Q10, and niacin, wherein the composition is administered in a concentration ranging from 10 to 20 mg/kg body weight. The present invention relates further to the composition for use in the treatment and/or prevention of radical and harmful forms of oxygen derived diseases, in particular of oxygen radical or reactive oxygen species derived diseases. The present invention relates further to the composition as a food supplement or dietary supplement.
CN101530420A Application of tunicamycin in preparing tumour cell reversing drug The invention relates to the technical field of medication. The tumour is always cured by operation, irradiation and chemical medication, and the induction differentiation therapy of malignant tumour becomes the research hotpot and frontier field of cancer biology and tumor therapeutics at present. The invention aims at providing a now application of tunicamycin which is the application in preparing a tumour cell reversing drug. The concentration of low-dosage tunicamycin adopted by the invention is 0.1-0.5mug/ml. After a myeloma cell line is treated, myeloma cell strain is differentiated in state, which is shown as cells are transited into mature plasma cell state; cell differentiation antigen CD49e is raised; and excreted immune globulin light chains are also increased. The invention has the advantages of low drug dosage of the tunicamycin, exact effect, less influence on normal cell and benefit for improving the living state of tumour patients.
CN103356688A Novel use of Polyflavanostilbene A in preparation of drugs for treating hemorrhagic fever with renal syndrome The invention discloses a novel use of Polyflavanostilbene A in preparation of drugs for treating hemorrhagic fever with renal syndrome. Hemorrhagic fever with renal syndrome virus in-vivo and in-vitro inhibition experiments prove that Polyflavanostilbene A has low cell toxicity, has effects of directly killing hemorrhagic fever with renal syndrome viruses and obviously inhibiting hemorrhagic fever with renal syndrome virus multiplication, has an obvious function of protecting a hamster infected by the hemorrhagic fever with renal syndrome viruses, delays disease time, prolongs a course of the disease and reduces a death rate. Therefore, Polyflavanostilbene A is an effective and safe drug for treating hemorrhagic fever with renal syndrome.
CN102861055A Application of Houttuynoid A in helicobacter pylori resisting medicine The invention relates to application of Houttuynoid A in helicobacter pylori resisting medicine. In-vitro activity experiments indicate that Houttuynoid A has strong helicobacter pylori (Hp) resisting activity. Houttuynoid A can be used for treating acute gastritis and chronic gastritis, gastric ulcer, duodenal ulcer and other diseases, can be applied for preparing medicine for treating acute gastritis and chronic gastritis, gastric ulcer, and duodenal ulcer. The application of Houttuynoid A in preparing the helicobacter pylori resisting medicine, which is provided by the invention, is disclosed for the first time. The skeleton type belongs to brand-new skeleton type, and the inhibiting activity of Houttuynoid A to helicobacter pylori is extremely strong, so that no possibility for providing any hint by other compounds exists. Houttuynoid A has outstanding actual characteristics. Meanwhile, Houttuynoid A has outstanding progress when being used for resisting helicobacter pylori infection.
WO2013171345A1 Tri-substituted glycerol compounds for use in the treatment of clinically isolated syndrome and/or multiple sclerosis The present invention relates to tri-substituted glycerol compounds according to formula (I) as described herein for use in the treatment of clinically isolated syndrome, relapsing remitting multiple sclerosis (RR-MS) and/or secondary progressive multiple sclerosis (SP-MS). The tri-substituted glycerol compounds according to formula (I) as described herein may also be used for the treatment of multiple sclerosis patients not adequately responding to interferon therapy. The present invention also relates to a tri-substituted glycerol compound as described herein, for use as a medicament, wherein the tri-substituted glycerol compound is administered in combination with at least one further pharmaceutically active compound.
US7084149 Anticancer agents; antitumor agents A composition containing a compound of the formula: wherein A is a nitrogen-containing heterocyclic group which may be substituted, R1 is a hydrogen atom, hydrocarbon group which may be substituted, or monocyclic aromatic heterocyclic group which may be substituted, R2 is a hydrogen atom or a lower alkyl group which may be substituted, R3, R4, R5, R6, R7, R8 and R9 are independently a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxy group which may be substituted, a thiol group which may be substituted, an amino group which may be substituted, an acyl group or a halogen atom, a salt thereof or a prodrug thereof has steroid C17,20-lyase inhibitory activity, and are useful for preventing and treating a mammal suffering from, for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.
US20100144776 Use of snps for the diagnosis of a pain protective haplotype in the gtp cyclohydrolase 1 gene (gch1) The present invention relates to an in vitro method for diagnosing a genetic predisposition or susceptibility for pain in a mammal which comprises detecting of at least one particular single nucleotide polymorphism (SNP) in a sample obtained from said mammal in the genomic locus-derived nucleic acid or fragment thereof of the locus GCH1.
US20080206219 Using cytokine modulators as therapeutic tools in treatment of vascular permeability disorders Methods, compounds and compositions for the modulation of TGF-β are disclosed wherein the vascular permeability in a subject is altered. The compounds can be antagonists or agonists, and can be oligonucleotides, antisense oligonucleotides, small molecules, antibodies, and the like. Compounds that modulate TGF-β, regulate TGF-β bioavailabililty, or the configuration and context of type 1 collagen can be used for the treatment or prevention of diseases caused by vascular permeability.
WO2012018854A8 Pactamycin analogs and methods of use Disclosed are pactamycin analogs, pharmaceutical compositions including the analogs, and methods of using the analogs, such as to inhibit tumor growth or a pathogenic infection such as a bacterial or parasitic infection. The pactamycin analogs have a general formula ( I ) where R1 is H, lower aliphatic, amide, acyl, or aminoacyl; R2 is -C(0)NR8 R9 where R8 and R9 independently are hydrogen or lower aliphatic, or R1 and R2 together form a cyclic structure; R3 and R4 independently are hydrogen, hydroxyl, or lower aliphatic, or R2 and R3 together form a cyclic structure; R5 is hydrogen or acyl; R6 and R7 independently are hydrogen, hydroxyl, halogen, lower aliphatic, or amino.
CN1864684A Lyophilized powder injection of doxofylline and preparation method thereof The present invention relates to doxofylline for treating asthma and its freeze dried powder for injection and preparation process. The freeze dried doxofylline powder for injection with high stability contains doxofylline as the active component and pharmaceutically acceptable solubilizer and excipient. The solubilizer may be one or several of methanesulfonic acid, maleic acid, glycine, citric acid, arinine, etc. and is preferably citric acid. The excipient may be one or several of mannitol, dextran, cyclodextrin and soluble starch, and is preferably mannitol. The injection of the present invention may be in different specifications containing doxofylline of 1-1000 mg, preferably of 50 mg, 100 mg, 150 mg, 200 mg, 300 mg, etc. The preparation process includes compounding medicine liquid, eliminating pyrogen, sterilizing, pouring, freeze drying and other steps.
CN1946407B Methods and composition for treating tumors and metastatic disease Compositions, methods, and combination therapies for the treatment of lymphomas, leukemias, melanomas, prostate cancer, and metastatic disease are provided. Specifically, compositions comprising anti-a4 integrin immunoglobulins or immunoglobulins that bind to an a4 integrin ligand (e.g., MadCAM-1 and VCAM-1) are disclosed for use in inhibiting tumor growth and progression and inhibition of metastases. A preferred immunoglobulin for use in treating tumors and metastases is natalizumab. The compositions and methods using these immunoglobulins can be used alone or in combination with other reagents and cancer treatment modalities.
US20100144698 Substituted azetidinones Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.
CN101708169A Colonic targeting administration preparation containing active substance of paeonol and preparation method thereof The invention discloses a recipe of a novel preparation containing paeonol and a preparation method. The invention solves colonic positioning medicine release by a method of combining a schardinger dextrin inclusion, an enzymolysis type substrate material and a coating. The preparation method comprises the following steps: mixing the paeonol or an inclusion compound thereof with a colonic enzymolysis type material and medicinal auxiliary materials which have a certain proportion, pressing the mixture into a tablet and preparing a tablet core; dissolving a coating material into an organic solvent, such as ethanol and propyl alcohol, adding a plasticizer, a viscosity resisting agent and a puffer, mixing evenly and coating the coating material on the tablet core by a coating of a fluidized bed so as to obtain the preparation. The enzymolysis type materials of the paeonol, pectin and the like are directly tabletted by powder, and the tablet with the weight percent being 0.5-30.0% and the diameter being 2-10mm in the tablet core is obtained. The recipe of the coating comprises one or more than two of the plasticizer and polyacrylic resin class coating materials with enteric solubility, and a coating layer is 3-30% of the weight of the tablet.
EP1670808A1 Antimicrobial derivatives Antimicrobial compounds are provided having the formula (Q): as well as tautomers, stereoisomers, pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
US20080207754 Method and apparatus for palatable prevention of acid reflux A method and applicators for preventing or reducing acid reflux (or “GERD”) by delivering a proper dose of vinegar directly to the back of the throat without exposing the taste buds, and immediately followed by a shot of water or other pleasant tasting chaser to wash it down. One applicator generally comprises a joined pair of sealed flexible pouches each sealed by a seal that may be burst open on the application of pressure to the pouches in order to dispense the product therein. The first pouch is filled with a dose of undiluted apple cider vinegar (approximately 5 to 10 cc) and the second pouch is filled with a liquid chaser, usually distilled water. Another applicator generally comprises a drinking vessel defined by two side-by-side receptacles, and pair of fixedly attached straws each entering a corresponding receptacle. The straw entering the chaser is oriented at a fixed angle greater than the straw entering the vinegar so that vinegar pours first followed by the chaser. In use, the vessel is lifted to the mouth with both straws disposed at the back of the throat, and the vessel is tilted so that the vinegar receptacle pours first, followed immediately by the chaser. This results in the vinegar pouring directly down the throat without exposing the taste buds, and being immediately followed by the chaser to wash it down.
US20050171070 Stable salts of o-acetylsalicylic acid containing basic amino acids II The present invention relates to improved compositions comprising stable salts of O-acetylsalicylic acid with basic amino acids, to pharmaceuticals comprising them and to their use for preparing pharmaceuticals.
CN103520142A Application of compound in preparing medicine for treating lung cancer The invention discloses an application of a compound in preparing medicine for treating the lung cancer and belongs to the technical field of medicine novel applications. The compound is Asperterpenols A, shows good lung-cancer-resistant activity and can be used for preparing the medicine for treating the lung cancer. The Asperterpenols A can remarkably inhibit the non-small cell lung cancer cells A549, the maxicell lung cancer cells NCI-H460, the lung squamous carcinoma cells HTB-8 and the human lung flat epithelium cancer cells QG-5, wherein the non-small cell lung cancer cells A549, the maxicell lung cancer cells NCI-H460, the lung squamous carcinoma cells HTB-8 and the human lung flat epithelium cancer cells QG-5 are cultured in vitro and the inhabitation effect on the human normal hepatocyte LO2 and the peripheral blood lymphocyte of the Asperterpenols A is small, and the obvious selecting performance is shown. The application of the Asperterpenols A in preparing the medicine for treating the lung cancer is disclosed for the first time and due to the fact that a framework type belongs to a totally novel framework type and the lung cancer cell inhibitory activity of the Asperterpenols A is high, the application has remarkable progress.
WO2008022535A1 A pharmaceutical composition for treating brain glioma, its process and pharmaceutical preparation A pharmaceutical composition for treating brain glioma, comprising temozolomide, borneol and/or menthol, wherein the weight rate of temozolomide: borneol and/or menthol is 1-50:2-100. The present invention also provides pharmaceutical preparation containing the above composition, and the process for the composition. The present pharmaceutical composition is very simple, and it has good curative effect and lower side effect, and the dose is also low.
US20120322886 Use of a saturated amines compound in manufacture of medicaments for mobilizing peripheral blood hematopoietic stem cell The invention provides a new use of a saturated amine compound, i.e., in manufacture of peripheral blood hematopoietic stem cell mobilizing agents. Experiments show that this compound (Code No. TA01) can efficiently mobilize hematopoietic stem cells into peripheral blood, and is a new type of hematopoietic stem cell mobilizing agents. The invention can play an important role in research and development of mobilizing agents for mobilizing hematopoietic stem cells into peripheral blood and has a promising application perspective.
US20080044439 Compositions and Methods for Preventing and Treating Skin and Hair Conditions The present invention discloses compositions and methods for the prevention and treatment of skin and hair diseases, such as, for example, alopecia, psoriasis, and keloids. The present invention also relates to compositions and methods for altering skin coloration. The present invention also relates to methods for enhancing the effect of a neurotoxin.
CN101485655B Application of dihydromyricetin in preparing medicament for preventing and treating adverse reaction of tumor chemoradiotherapy The invention discloses application of dihydromyricetin in preparing a medicine for preventing and treating untoward reactions in radiotherapy and chemotherapy of tumor. In particular, the application is to prepare medicines for preventing and treating untoward reactions in radiotherapy and chemotherapy of tumor, preventing and treating arrest of bone marrow and baldness, resisting mutation, preventing and treating the generation of secondary tumors, preventing and treating tumor transfer, and preventing and treating breast cancer, cervical carcinoma, intestinal cancer and the like. The invention creatively finds that the dihydromyricetin has the effects of removing free radicals, inhibiting reaction chains of the free radicals, resisting the mutation, inhibiting the expression of the tumor gene, causing the death of tumor cells, preventing and treating the tumor generation, preventing and treating the secondary tumors and the transfer of the secondary tumors and preventing and treating infection. Therefore, as the medicine for preventing and treating untoward reactions in radiotherapy and chemotherapy of tumor, the dihydromyricetin can inhibit and alleviate chemical damage, prevent and treat damage of a mutagen and further prevent gene mutation or the secondary tumors; and by combination with the radiotherapy and chemotherapy, the effects of preventing untoward reactions in radiotherapy and chemotherapy of tumor and preventing generation of tumors are achieved.
US20090093469 Phenylaminopropanol Derivatives and Methods of Their Use The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
CN101757252A Method for preparing volatile oil for Jingfukang preparation The invention discloses a method for preparing volatile oil for Jingfukang preparation, which relates to the technical field of medicine. The method comprises the following steps of: (1) adopting an extracting-rectifying coupled device for extraction; (2) adopting a two-step extraction technology: (a) adopting an extracting-rectifying coupled technology to extract the volatile oils of four medicinal materials including notopterygium root, frankincense, myrrh and rhizoma atractylodis; and (b) adopting the extracting-rectifying coupled technology to extract the volatile oil of hemlock parsley. During the process for extracting the volatile oils of the five medicinal materials, the four medicinal materials of notopterygium root, frankincense, myrrh and rhizoma atractylodis are extracted in a mixed mode, and the medicinal material of hemlock parsley is individually extracted. The invention has the advantages that the oil yield of the volatile oil for Jingfukang preparation is high, ligustilide which is the characteristic component of the volatile oil of the medicinal material of hemlock parsley can be detected, so that the volatile oil of the medicinal material of hemlock parsley can be fully utilized, which provides a solid foundation for the exertion of the effect of the Jingfukang preparation; moreover, the method solves the problems that the prior art has low oil yield of the volatile oil and can not fully extract ligustilide which is the characteristic component of the volatile oil of hemlock parsley.
WO2012154274A1 Triazolopyridine compounds as pim kinase inhibitors Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.
US20120277270 Method for Decreasing Symptoms of Alcohol Consumption The present invention relates to methods and compositions of metadoxine and physiologically compatible active derivatives thereof, and their use for decreasing symptoms of alcohol consumption as well as in the prevention of alcohol consumption related symptoms in subjects in need thereof.
US20100076079 Pharmaceutical Compositions Of Short-Acting Sedative Hypnotic Agent The invention provides pharmaceutical compositions comprising a phenylacetic acid ester compound useful for inducing or maintaining general anesthesia or sedation in mammals, methods for preparing such compositions, and methods for inducing or maintaining anesthesia or sedation using such compositions.
US20110274726 Chitosan foam medical devices and methods The invention provides a solid foam wound dressing useful for hemorrhage control and wound repair, as well as methods for making such a wound dressing.
WO2010131038A3 Steroid containing composition and uses thereof The present invention provides the use of a steroid in combination with an anti-oxidant or an inhibitor of forkhead signalling, in particular, for the treatment, amelioration or prevention of tissue degeneration and/or pain and/or inflammation and/or for facilitating tissue repair. The invention also provides a composition comprising a steroid and an anti-oxidant or an inhibitor of forkhead signalling.
US20050288351 Azaspiro compounds for the treatment of pain This invention relates to azaspiro compounds and their use as medications especially for the treatment of chronic, chronic-phlogistic and/or neuropathic pain. A compound that lends itself particularly well to the production of analgesics is 2-azaspiro[4.6]undecane-3-thion.
WO2014031792A3 Methods of treating epilepsy or status epilepticus Described herein are methods of treating epilepsy or status epilepticus, e.g., convulsive status epilepticus, e.g., early status epilepticus, established status epilepticus, refractory status epilepticus, super-refractory status epilepticus, e.g., super-refractory generalized status epilepticus; non- convulsive status epilepticus, e.g., generalized status epilepticus, complex partial status epilepticus; generalized periodic epileptiform discharges; periodic lateralized epileptiform discharges; a seizure, e.g., acute repetitive seizures, cluster seizures, the method comprising administering to the subject a neuroactive steroid.
CN102342913A Intra-intestinal nutrient emulsion for tumor patients and preparation method thereof The invention relates to an intra-intestinal nutrient emulsion for tumor patients and a preparation method thereof, belonging to the technical field of nutrient medicament preparation. The intra-intestinal nutrient emulsion is prepared by preparation of primary emulsion, dilution, storage, packaging, and sterilization. The intra-intestinal nutrient emulsion contains protein, fat, carbohydrates, vitamins, minerals, microelements, dietary fibers and other nutrients. The energy distribution of the intra-intestinal nutrient emulsion is as follows: 18% of protein, 50% of fat and 32% of carbohydrates, thereby increasing the energy supply ratio of fat and reducing the energy supply ratio of carbohydrates. The intra-intestinal nutrient emulsion is designed according to the tumor patients and meets the metabolism need of the tumor patients. The whole production process of the emulsion is carried out under nitrogen protection, and through sterilization of a rotary sterilization kettle, the effective ingredients of the product can be better retained.
US20110053845 Localized vaginal delivery without detrimental blood levels The invention relates to a pharmaceutical composition for vaginal administration of a treating agent normally associated with undesired side effects at detrimental blood levels. The composition releases the treating agent at a rate to achieve local tissue concentrations without such detrimental blood levels by using a therapeutically effective amount of the treating agent and a bioadhesive, cross-linked water swellable, but water-insoluble polycarboxylic acid polymer. Using this composition and the method of treatment provides sufficient local levels of the drug to provide therapeutic efficacy, but avoids many untoward adverse events. The invention also relates to a pharmaceutical composition for use during menses that includes a treating agent and a bioadhesive, cross-linked water swellable, but water-insoluble polycarboxylic acid polymer.
CA2197628C Substituted thiophenylalkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them Substituted thiophenylalkenylcarboxylic acid guanidides, processes for their preparation, their use as a medicament or diagnostic, and a medicament containing them.There are described substituted thiophenylalkenylcarboxylic acid guanidides of the formula I in which R(1) to R(5) have the meanings given in the claims, which are outstandingly active antiarrhythmic pharmaceuticals having a cardioprotective component and are outstandingly suitable for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they also inhibit or greatly reduce the pathophysiological processes in the formation of ischemically induced damage, in particular in the initiation of ischemically induced cardiac arrhythmias, in a preventive manner.
CN101781268B Isothiazole ketone substituted benzene dicarboxylic acid derivative and usage thereof in preparation of beta-secretase inhibitor The invention relates to an isothiazole ketone substituted benzene dicarboxylic acid derivative and the usage thereof in preparation of beta-secretase inhibitor. More particularly, the invention relates to a compound in formula I or II, or possible isomer, prodrug, pharmaceutical salt, solvent complex or hydrate, wherein symbols are described in specification. The invention further relates to a preparation method, a pharmaceutical composition containing the compound, and the usage of the compound in the preparation of medicine for treating and/or preventing diseases or symptoms relating to beta-amyloid peptide aggregation or settlement. The compound can be used as the beta-secretase inhibitor.
EP1492569A4 Aqueous dispersible steryl ester compositions The present invention relates to water dispersible steryl ester compositions that include steryl esters, an emulsifier, and a protein or lipophilic starch stabilizer. Such compositions of the invention can be incorporated into aqueous foods and beverages.
WO2014005224A1 Quercetin-3-glucoside and uses thereof There is described herein a use of quercetin-3-O-β-D-glucoside (Q3G) for increasing the amount of cell surface low-density lipoprotein receptor (LDLR) on a cell and for reducing the amount of functional proprotein convertase subtilisin/kexin type 9 (PCSK9) secreted by the cell, where the Q3G is formulated for administration to the cell, and where the increase in cell surface LDLR and the decrease in secretion of functional PCSK9 is in comparison to the cell not exposed to Q3G. The use may optionally include the treatment of a statin. There is also described a method of reducing plasma cholesterol levels in a patient in need thereof. The method includes treating the patient with a therapeutically effective amount of Q3G and, optionally, a therapeutically effective amount of a statin.
WO2009056693A1 Novel derivatives of n, n'- 2, 4-dianilinopyrimidines, preparation thereof as medicaments pharmaceutical compositions and in particular as ikk inhibitors The invention relates to products of formula (I): said products being in all isomeric forms and all salts as medicaments, particularly as IKK inhibitors.
CN101724021A Polypeptide conjugates of taxol or docetaxel The invention discloses a series of polypeptide conjugates of taxol or docetaxel. The taxol or docetaxel is connected with polypeptide amino groups in 2' position hydroxyl group through different connection sequences.The invention also discloses a preparation method and applications of the conjugates in preparing medicaments. The conjugates of the invention have the advantages of excellent anti-cancer activity, cancer cell selectivity and water solubility.
US20050123671 Incorporating trehalose into an edible aqueous system containing alpha glucosyl hesperidin or catechin or both followed by sterilization A reduction inhibitory agent for active oxygen eliminating activity which comprises cyclotetrasaccharide i.e., cyclo{6}-α-D-glucopyranosyl-(1 3)-α-D-glucopyranosyl-(1 6)-α-D-glucopyranosyl-(1 3)-α-D-glucopyranosyl-(1), as an effective ingredient, a method for inhibiting the reduction of active oxygen eliminating activity which comprises incorporating either cyclotetrasaccharide or the reduction inhibitory agent into plant edible products and/or plant antioxidants, and a composition where the reduction of active oxygen eliminating activity of the plant edible products and/or plant antioxidants has been satisfactorily inhibited by the method.
CN102702298A Glycyrrhetinic acid derivative and preparation method and medical application thereof The invention relates to the medicine field, in particular to a glycyrrhetinic acid derivativeor pharmaceutically acceptable salt thereof, preparation methods of the glycyrrhetinic acid derivative and the salt of the glycyrrhetinic acid derivative thereof, a medical composition containing the glycyrrhetinic acid derivative, and medical application of the glycyrrhetinic acid derivatives and pharmaceutically acceptable salt thereof, wherein the glycyrrhetinic acid derivative and the pharmaceutically acceptable salt thereof are represented by formulas (I, II and III). Pharmacological experimental results show that the compound has excellent anti-inflammatory, anti-tumor and hypoglycemicactivity, and can be used for preparing medicines for treating inflammatory diseases, tumors and diabetes mellitus.
CN101548979A New medicine combination for treating enteritis and bacillary dysentery The invention discloses a new medicine combination for treating enteritis and bacillary dysentery, comprising the main components of gentamicin sulphate and tannin matrine. The compatibility of the medicine of the new medicine combination is as follows: 1mg (1 kilounit according to the gentamicin) to 400mg (0.4 megaunit according to the gentamicin) of gentamicin sulphate, 10mg (1.5mg according to the matrine) to 3,000mg (440mg according to the matrine) of tannin matrine, and the two medicines are combined together to be used for treating bacillary dysentery, enteritis, and laxness caused by various infections in intestinal tracts according to any proportion, and also treating ulcerative colitis, irritable bowel syndrome and other functional diarrheas. The invention can be also applied to solve the problem of exhaustion of resources by using the tannic acid matrine of a renewable resource to replace basic bismuth carbonate of bismuth metal of raw materials of a non-renewable resource.
CN1628654A Liver benefiting effective agent prepared from hepadestal and preparation method thereof The invention provides a liver benefiting effective agent prepared from hepadestal and preparation method, wherein preparation include various dosage types including dispersion tablet, capsule, ball and drop pills prepared from hepadestal. The obtained medicament has the functions of improving liver functions, and protect hepatocyte membrane, it can be applied to the treatment of acute and chronic hepatitis.
US6852335 Folic acid in solid dosage forms A nutritional tablet or caplet has a film coating that contains folic acid available for rapid release upon contact with gastric fluid. The film coating also includes a film forming polymer such as hydroxypropyl methylcellulose.
CN102727499A Application of compound 6-furfurylaminopurine in preparations of anti-vascular dementia drugs The present invention discloses an application of a compound 6-furfurylaminopurine in preparations of anti-vascular dementia drugs. The study results show that the 6-furfurylaminopurine can play animal and plant hormone-like effects, and can directly capture and remove excess free radicals in brain tissues; with the 6-furfurylaminopurine, cerebral hypoperfusion during a cerebral ischemia process can be significantly increased, the brain infarction volume can be reduced (and a dose-response relationship exists), and neuroethology injury symptoms after ischemia-reperfusion can be significantly improved. In addition, with the 6-furfurylaminopurine, cognitive dysfunction induced after rat cerebral ischemia can be improved, brain tissue antioxidase synthesis can be prompted, activity of the brain tissue antioxidase can be improved, and exogenous and endogenous oxidative damage resistance of the brain tissue can be improved so as to protect the integrity of the structure and the function of brain cells, and maintain the normal physiological function of the brain tissue. The compound 6-furfurylaminopurine of the present invention is a compound for effective treatment of vascular dementia and having development prospects.
US20090004140 4-substituted pyrrolidine as anti-infectives The present invention discloses compounds of Formulae (I) and (II), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
CA2638622A1 Peripheral and neural inflammatory crosstalk Disclosed are compositions and methods for the study and treatment of inflammatory disease, neurological disorders, bone disease, pain, and methods of making and using thereof.
CN101536974A Eye methazolamide temperature-sensitive situ-gel preparation and preparation method thereof The invention relates to an eye methazolamide temperature-sensitive situ-gel preparation, prescription components and weight percentage content are as follows: 0.01-1 percent of active ingredient, 10-40 percent of gel matrix, 0.001-0.2 percent of antiseptic, 1-10 percent of osmotic pressure regulator, 0.1-5 percent of tackifier, pH regulator, and the balance ultra-pure water, wherein pH value of solution is adjusted to be 5.0-8.0. The pharmacodynamics result shows that the eye methazolamide temperature-sensitive situ-gel preparation has better and more durable intraocular pressure reduction effect compared with brinzolamide eye drops in the market. The eye methazolamide temperature-sensitive situ-gel preparation has better biocompatibility without stimulating eyes; the rheology result shows that the preparation method has characteristics of pseudoplastic fluid, reduces the viscosity along with the increment of the shearing force, i.e. the viscosity is reduced when in blinking, and the viscosity is restored when not in blinking, and the defects of fatness of cream and the like and dimness of vision can not be produced, therefore, the invention increases the adaptability of a patient.
US6995261 Treatment of meningitis, septic shock, infections, reperfusion injuries, hepatitis, pancreatitis; bone, autoimmune, viral, and respiratory system disorders; antiinflammatory, antiarthritic, and antitumor agents Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0–6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1β protease activity in a mammal utilizing the compounds and compositions.
CN103145583A Raceme alkannin naphthazarin parent nucleus hydroxyl methylation carbonyl oxime derivative and preparation and application thereof The invention discloses a raceme alkannin naphthazarin parent nucleus hydroxyl methylation carbonyl oxime derivative, and preparation and application thereof. The structural formula of the derivative is showed in a formula (I) or a formula (II), wherein, R1 or H is alkane or olefin or arene or replacing arene of six carbon atoms, and R2 or H is alkane of the six carbon atoms. The preparation of the compound has the advantages that raw materials are easy to obtain, a preparation method is simple, a yield coefficient is high, and the like; the prepared raceme alkannin derivative achieves shikonin naphthazarin parent nucleus hydroxyl methyl carbonyl oximation, and the structure is novel; and at the same time, experimental results of antitumor activity in vitro show that the compound is good in antitumor activity.
CN101357134A Potenciador del efecto antitumoral y agente antitumoral Provided is an antitumor effect potentiator containing a therapeutically efficacious amount of Tegafur, Gimeracil in an amount efficacious for potentiating the antitumor effect and Oteracil potassium in an amount efficacious in inhibiting side effects, characterized by containing at least one component selected from the group consisting of folinic acid and its pharmaceutically acceptable salts in an amount efficacious for potentiating the antitumor effect as the active ingredient; an antitumor agent characterized by containing a therapeutically efficacious amount of Tegafur, Gimeracil in an amount efficacious for potentiating the antitumor effect and Oteracil potassium in an amount efficacious in inhibiting side effects and , together with at least one component selected from the group consisting of folinic acid and its pharmaceutically acceptable salts in an amount efficacious for potentiating the antitumor effect as the active ingredient; a method of potentiating the antitumor effect of an antitumor agent characterized by comprising administering the above-described antitumor effect potentiator to a patient; and a method of treating cancer characterized by comprising administering the above antitumor agent to a patient.
CN101947226A Drops for treating pink eye The invention discloses drops for treating pink eye. The drops can be prepared from the following steps of: selecting dexamethasone with unit of 0.5ml:1mg, epinephrine injection with unit of 1ml:1ml, injection liquid of gentamicin with unit of 40,000 to 80,000 and berberine, wherein the volumes of the dexamethasone, the epinephrine injection, the injection liquid of gentamicin and the berberine are the same; and mixing 1 to 2 of each of the four injections and 0.5 to 3g of borneol. The pink eye can be treated by dripping the drops for treating the pink eye on an affected part, three times each day. The drops have the effects of improving eyesight, sterilizing and diminishing inflammation and clearing away heat and toxic material.
CN102391305A Phosphate disodium salt hydrate of propofol hydroxyacid ester and preparation method and application thereof The invention relates to a phosphate disodium salt hydrate of propofol hydroxyacid ester and a preparation method and application thereof. The structure of the hydrate is shown as a formula (I), wherein x in the formula is an integer from 1 to 10. The hydrate can rapidly release propofol with a sedativehypnotic and/or anesthetic effect in the blood plasma and is not apt to be dampened, the stability is good, the quality is easy to control, the problems that water content is difficult to control and a quality standard is difficult to draw up because the hygroscopic property of the existing phosphate disodium salt compound is strong and the large-scale industrialized production is realized.
CN101810602A Application of compound 3,5,2',4'-tetrahydroxy chalcone in preparation of drug for preventing and treating hyperuricemia and gout The invention discloses application of a compound 3,5,2',4'-tetrahydroxy chalcone in preparation of a drug for preventing and treating hyperuricemia and gout, relating to the application of drugs containing organic components. The compound obviously inhibits the activity of xanthine oxidase in vitro, wherein IC50 has the dosage of 22.5 mu mol/L and is a competitive inhibitor. In-vivo research shows that the compound has stronger gout resistant role, can obviously lower the uric acid level of serum of a rat with hyperuricemia induced by potassium oxonate or hypoxanthine by using 14.6 mu mol/kg (3.98mg/kg) dose, has less toxic and side effects, the maximum tolerance dose for intragastric administration of the rat being 5.0g/kg and obviously lower toxicity than gout resisting drugs used clinically at present, such as allopurinol, colchicin, benzbromarone, and the like, and can be used for preparing drugs and health care products for preventing and treating hyperuricemia and gout.
CN101849951A Medicinal composition used for resisting HIV virus The invention discloses a medicinal composition used for resisting an HIV virus. The medicinal composition is composited by an active ingredient which is formed by tailifovir and other one or more of reverse transciptase inhibitors, and suitable excipient. The reverse transciptase inhibitors comprise nucleoside inhibitors and non-nucleoside inhibitors. The composition can be prepared into oral preparations which comprise troches, capsules, dispersible tablets, chewable tablets, orally disintegrating tablets, buccal tablets, pills, soft capsules and the like used for treating acquired immune deficiency syndrome.
US20050187212 Pharmaceutical composition for topical delivery of meloxicam A pharmaceutical composition comprising: (a) a pharmaceutically effective amount of meloxicam, or a pharmaceutically acceptable salt thereof; (b) a skin permeation enhancing agent selected from the group consisting of: (i) an amine of formula I wherein: R1, R2, and R3 are each independently an alkanolyl group with 1 to 24 C-atoms, in which one or more H-atoms are optionally substituted by —OH and/or one or more —CH2— groups are optionally substituted by —O—, or a polyoxyethylene group with 2 to 30 ethylene oxide units, and R2 and R3 are additionally independently H or a linear, branched, or cyclic alkyl group with 1 to 24 C-atoms, in which one or more —CH2— groups are optionally substituted by —CH═CH— and/or —O— and/or in which one or more H-atoms are optionally substituted by —OH, and (ii) an amide of formula II wherein: R4 and R5 are each independently a linear, branched, or cyclic alkyl group with 1 to 24 C-atoms, in which one or more —CH2— groups are optionally substituted by —CH═CH—and/or —O— and/or in which one or more H-atoms are optionally substituted by —OH, and R6 is H or a linear, branched, or cyclic alkyl group with 1 to 24 C-atoms, in which one or more —CH2— groups are optionally substituted by —CH═CH— and/or —O— and/or in which one or more H-atoms are optionally substituted by —OH; and (c) at least one inert carrier. Furthermore this invention relates to a transdermal delivery system and a method for treating, preventing and/or relieving the signs and/or symptoms of rheumatoid arthritis, cervico-omo-brachial syndrome, low back pain, osteoarthritis, periarthritis scapulohumeralis, tendovaginitis, peritendinitis, humerus epicondylitis, including tennis elbow, myalgia, post-traumatic tumor and pain.
WO2008104472A1 2, 4 -diaminopyrimidine derivatives and their use as p2x antagonists or as prodrugs thereof Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the compounds being of formula (I): wherein R1, R2, R3 and R4 are as defined herein.
EP1105370B9 Novel aryl sulphonamides and analogues The present invention relates to novel aryl sulphonamides and analogues, methods for the production and use thereof in the prophylaxis and treatment of neurodegenerative diseases, especially in the treatment of apoplexia cerebri, craniocerebral trauma, pain and spasticity.
US20110053950 4-benzylidene-3-methylpiperidine aryl carboxamide compounds useful as faah inhibitors The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or heteroaryl; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.
US20110086829 Compositions and methods for treating obesity Compositions and methods for treating obesity in a subject are described. Some embodiments provide methods for administering pharmaceutical formulations including biocompatible emulsifiers in an amount effective to treat obesity. In some embodiments, pharmaceutical formulations include a combination of two or more biocompatible emulsifiers effective to treat obesity.
EP1237545B1 Use of stearidonic acid in the manufacture of a medicament for the treatment or prevention of cancer Cancer in a mammal can be treated or prevented by administering to a mammal in need thereof a cancer inhibiting amount of metabolite(s) of α-linolenic acid, such as stearidonic acid (18:4 n-3), eicosatetraenoic acid (20:4 n-3), docosapentaenoic acid (22:5 n-3) and mixtures thereof, especially metabolites including stearidonic acid.
CN101259126A Composition for treating hyperlipidemia and preparation thereof The invention provides a novel medicinal composition for treating hyperlipidemia and a preparation method thereof, and relates to the medicine technical field. The medical composition is characterized by containing effective dose of anethol trithione and stantins, with a weight proportion of 0.5-20: 1 and a preferential weight proportion of 1-5: 1, and can be prepared into all pharmaceutically acceptable dosage forms. The combination of the anethol trithione and the stantins has a lipid lowering function obviously better than that of a single medicine, which reveals that combination of the two medicines has synergistic effect without obvious toxic action.
CN1981739B Esmolol preparation An aqueous, sterile pharmaceutical composition suitable for parenteral administration for the treatment of cardiac conditions, comprising methyl-3-[4-(2-hydroxy-3-isopropylamino) propoxy] phenylpropionate hydrochloride (esmolol hydrochloride), a buffering agent and an osmotic-adjusting agent, as well as a method for its manufacture, are disclosed.
WO2007098086A3 Hydroxypiperidine derivatives and uses thereof Chemical agents, such as derivatives of hydroxypiperidine moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
WO2009069668A1 Agent for increasing the expression of malignant melanoma antigen, and use thereof Disclosed is a means which is effective for the treatment of melanoma. Specifically disclosed is an agent for increasing the expression of a malignant melanoma antigen, which comprises a compound selected from the group consisting of methotrexate, paclitaxel, daunorubicin hydrochloride (daunorubicin, HCl), doxorubicin hydrochloride (doxorubicin, HCl), actinomycin D, camptothecin, etoposide, cytochalasin D, 3-ATA (3-amino-9-thio(10H)-acridone), aphidicolin, bisindolylmaleimide I, an arabino nucleoside (cytosine arabinoside), curcumin, 2',3'-dideoxythymidine triphosphate (2',3'-dideoxythymidine 5'-triphosphate), a thymidine dimer (dipyrimidine dithymidylic acid), pyridoxal phosphate (pyridoxal 5'-phosphate hydrate), epigallocatechin gallate ((-)-epigallocatechin gallate), vidarabine, resveratrol and lithocholic acid.
WO2006050458A2 Tadalafil crystal forms and processes for preparing them The present invention provides tadalafil crystal forms II, III, IV, VI, VII, and VIII, and processes for preparing these forms. The present invention also provides processes for preparing tadalafil forms I and V.
CN101544662A Cefotiam salt compound and pharmaceutical composition made therefrom The invention relates to a high-purity cefotiam hydrochloride compound prepared from crystal cefotiam or a crude product of crystal cefotiam salt. The invention also relates to a product obtained according to a purification method of the invention, in particular to a pure cefotiam hydrochloride and a pharmaceutical composition containing the product.
CN103652128A Radix paeoniae rubra health tea for improving eyesight and relieving pain The invention relates to radix paeoniae rubra health tea for improving eyesight and relieving pain. The radix paeoniae rubra health tea for improving eyesight and relieving pain is prepared by the following steps: putting 24 parts of radix paeoniae rubra, 11 parts of borneol, 13 parts of rhizoma zingiberis, 15 parts of felwort, 14 parts of ephedra, 12 parts of cape jasmine and 11 parts of mint into a frying pan; boiling in water with weight being 70 times of that of the total weight of all the materials put in the frying pan for 15 minutes, and then filtering by a 30-mesh gauze to obtain filtrate A; pouring the filtrate A into the frying pan, and adding water with weight being 1.5 times of that of the filtrate A for boiling for 20 minutes, and then filtering by the 30-mesh gauze to obtain filtrate B; distilling and concentrating into 1/3 of original volume after mixing the filtrate A with the filtrate B, so as to form dilute tea cream; filtering, distilling and drying again, so as to prepare the radix paeoniae rubra health tea for improving eyesight and relieving pain. The radix paeoniae rubra health tea for improving eyesight and relieving pain disclosed by the invention is simple in preparation method, fresh and delicious, and aromatic in smell, has the effects of relieving swelling and pain and removing nebula, and can help people relieve eye fatigue after being drunk for a long period of time, so that the symptom of eye ache is reduced.
CN102793777A Groundsel garden burnet pain relieving powder The invention discloses groundsel garden burnet pain relieving powder, which is the latest product. The groundsel garden burnet pain relieving powder is prepared from garden burnet powder, groundsel and magnesium chloride. The product can diminish inflammation and relieve pain and can prevent and treat various harmful germ infections; and therefore, the product can prevent various innominate inflanunatories of unknown origins, such as malignant boil, furuncle and carbuncle, and various diseases.
US20110038954 Calcium-rich alkaline power produced from processed mollusc shells A calcium-rich powder possessing therapeutic properties produced by washing and sterilising the shells of molluscs taken from an uncontaminated marine environment, heating said washed and sterilised shells to a temperature of between 1000° C. and 2000° C. for a period of at least 10 hours, reducing the temperature of the resultant material to room ambient temperature over a period of at least 24 hours, and then crushing said resultant material to a fine powder.
DE102009051066A1 Composition, useful for preparing a drug for treating e.g. limbs-, tendon-, muscle pain, comprises a carrier medium, menthol, horse chestnut seed extract, white willow bark extract, Arnica tincture, rosemary oil and St. John's wort oil Composition comprises: a carrier medium a carrier medium, menthol (0.1-1 wt.%), horse chestnut seed extract (1-5 wt.%), white willow bark extract (1-5 wt.%), Arnicatincture (2-8 wt.%), rosemary oil (0.25-5 wt.%) and St. John's wort oil (1-5 wt.%). - ACTIVITY : Analgesic; Antirheumatic. No biological data given. - MECHANISM OF ACTION : None given.
EP1510223A1 Intravenous composition, process for producing the same and preparation thereof A composition for intravenous injection, which is gradually decomposed instead of fat particles, has sufficient sustained release effects, has an excellent encapsulation ratio of lipid-soluble agents, and has such sustained release effects at lesion sites; a production method thereof; and a preparation containing the composition. The composition for intravenous injection is produced by encapsulating a prostanoid or steroid in a poly(lactic-co-glycolic acid) or poly(lactic acid) microparticle, and allowing lecithin or similar surfactant to be adsorbed on the surface of the above poly(lactic-co-glycolic acid) or poly(lactic acid) microparticle. A method for producing the composition comprises: dissolving esterified prostanoic acid or esterified steroid and a poly(lactic-co-glycolic acid) or poly(lactic acid) in an organic solvent such as dichloromethane or dimethylsulfoxide; and emulsifying the obtained mixture in water, using the lecithin or similar surfactant capable of adjusting the diameter of the copolymer or particle to between 50 and 500 nm, employing an ultrasonic generator, a Polytron Homogenizer, or the like.
US7300927 Method for treating or preventing Alzheimer's disease Disclosed is a method for treating or preventing Alzheimer's disease by restricting the level of metabolizable carbohydrate in the diet and/or administering to the patient an effective amount of an agent which reduces serum insulin levels.
US7482439 Caprazene as novel compound and derivatives thereof, and caprazol as novel compound and derivatives thereof Caprazene and caprazol could be synthesized by hydrolysis of a caprazamycin. There could be synthesized a caprazene-1′″-amide derivative of the formula (II) and a caprazene-1′″-ester derivative of the formula (III) from caprazene. Further, there could be synthesized a caprazol-1′″-amide derivative of the formula (V) and a caprazol-1′″-amide-3′″-ester derivative and a caprazol-3′″-ester derivative, etc. from caprazol. Furthermore, an imidazolidinone derivative could be synthesized from the ring-opened product of the 1,4-diazepinone ring of caprazol. The novel caprazene derivative, novel caprazol derivative and novel imidazolidinone derivative now synthesized exhibit excellent antibacterial activities against a variety of bacteria, including acid-fast bacteria.
US20110294732 Erythropoletin complementation or replacement The present invention provides methods and compositions to replace up to 90% of erythropoietin use in the treatment of anemias and hypoxias. The method employs acid and salt forms of inositol-tripyrophosphate (ITPP) isomers to shift the P50 value of hemoglobin, thereby improving the rate and efficiency of oxygenation by blood even when red blood cell counts are low. Indications for the new method include anemias and hypoxia arising from infection, chemotherapy, premature birth, altitude change, compromised lung or heart function, aplastic anemia and anemia associated with a myelodysplastic syndrome, and other causes.
US20090074710 Method of treatment using a cytokine able to bind il-18bp to inhibit the activity of a second cytokine The present invention relates to the use of a cytokine-1, preferably from the IL-1 family more preferably IL-1F7b, or an isoform, mutein, fused protein, functional derivative or fragment thereof capable of binding to IL-18BP or a mutein, fused protein, functional derivative or fragment thereof and capable of inhibiting a receptor of a cytokine-2, cytokine-2 being a member of the IL-1 family, preferably IL-18, in the manufacture of a medicament for the treatment or prevention of a disease which is caused or aggravated by inducing said receptor of cytokine-2.
WO2006054770A1 Novel map kinase kinase kinase (mapkkk) It is intended to provide a novel MAPKKK in humans and mouse. It is also intended to provide a preventive/remedy having an improved safety and an elevated efficacy for an apoptosis-associated disease by inhibiting the novel MAPKKK in humans or mouse. Namely, a novel protein originating in humans or mouse which serves as MAPKKK is provided. Further, it is indicated that the JNK/p38 signal transduction pathway is inhibited or promoted and thus apoptosis can be promoted or suppressed in an apoptosis-associated diseases by inhibiting or promoting the kinase activity of the above protein. Thus, the disease can be treated/prevented thereby. Consequently, a medicinal composition containing an agent capable of inhibiting or promoting the kinase activity of the above-described novel protein is provided.
WO2009027730A1 Quinolin-4-one and 4-oxodihydrocinnoline derivatives as inhibitors of poly(adp-ribose)polymerase (parp) The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP- ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo-or radiosensitizers for cancer treatment.
WO2011030798A1 8-oxodihydropurine derivative A compound represented by formula (1) or a pharmaceutically acceptable salt thereof (in the formula, W represents a hydrogen atom, a halogen atom, or the like; A represents an alkyl group which may be substituted by an aryl group or the like, an aryl group, or the like; and one of X and Y represents a di-substituted alkylaminocarbonyl group, or the like, and the other represents a hydrogen atom, an alkyl group, an alkylcarbonyl group, or the like); a medicinal agent or a pharmaceutical composition for treating or preventing FAAH-related diseases such as depression, anxiety and pains, which comprises the compound or the like as an active ingredient; use of the compound or the like; and a treatment or prevention method.
US20100136010 Novel 27875, 22025, 27420, 17906, 16319, 55092 and 10218 molecules and uses therefor The invention provides isolated nucleic acids molecules, designated 27875, 22025, 27420, 16319, 55092 and 10218 nucleic acid molecules. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing 27875, 22025, 27420, 16319, 55092 and 10218 nucleic acid molecules, host cells into which the expression vectors have been introduced, and nonhuman transgenic animals in which a 27875, 22025, 27420, 16319, 55092 and 10218 gene has been introduced or disrupted. The invention still further provides isolated 27875, 22025, 27420, 17906, 16319, 55092 or 10218 proteins, fusion proteins, antigenic peptides and anti-27875, 22025, 27420, 17906, 16319, 55092 or 10218 antibodies. Diagnostic and therapeutic methods utilizing compositions of the invention are also provided.
US20110071215 Compositions and methods for diagnosis, prognosis and treatment of mesothelioma Described herein are compositions and methods for the diagnosis and treatment of mesothelioma patients and the prognosis of mesothelioma patients after surgical operation. Specifically the invention relates to microRNA molecules associated with diagnosis, treatment and prognosis of mesothelioma, as well as various nucleic acid molecules relating thereto or derived therefrom.
CN102133224A Compound Iansoprazole chewable tablets The invention relates to chewable tablets of a compound Iansoprazole pharmaceutical composition, which is prepared from Iansoprazole, sodium bicarbonate, magnesium hydroxide and special excipients for preparing chewable tablets pharmaceutically. According to the invention, the disintegration time limited, dissolution rate and taste of the compound Iansoprazole chewable tablets are better than that of other products in the prior art, unexpected technical effects are obtained, the product quality of the preparation is improved, and the toxic side effects are reduced.
WO2013161821A1 Cgrp responsiveness promoter Provided is a substance that can promote the CGRP responsiveness of cells. Lignans represented by formula (I) (in the formula (I), R1 represents a hydrogen atom or an alkoxy group, and R2, R3 and R4 which may be the same or different each represent an alkoxy group) are used for promoting CGRP responsiveness of cells.
CA2305331C Methods for decreasing the frequency of transmission of viral and for preventing and treating bacterial infections using cellulose acetate phthalate or hyroxypropyl methylcellulose phthalate excipients A method for decreasing the frequency of transmission of human immunodeficiency virus or herpesviruses or for preventing the transmission of or treating a sexually transmitted bacteria] infection by administering to a human an anti-human immunodeficiency virus amount or an anti-herpesvirus amount or an anti-bacterial amount of cellulose acetate phthalate (CAP) or hydroxypropyl methylcellulose phthalate (HPMCP), such as in micronized form, or a combination thereof, either alone or in combination with a pharmaceutically acceptable carrier or diluent. The CAP and/or HPMCP may be employed as a suspension of micronized particles and may further contain a water miscible, non-solvent for CAP or HPMCP, such as glycerol.
US20120149775 Methods for preventing and improving skin elastic property loss The present invention is directed to method for preventing and improving an aggravation of a skin condition accompanied with a skin elastic property loss by suppressing an increase in, or inhibiting the physiological activity of, palmitic acid. The present invention provides a cosmetic method for preventing and improving wrinkling and sagging accompanied with a skin elastic property loss and a method for preventing and treating a wound healing disorder and a bedsore.
EP0946499B1 N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions. Said compounds are represented by formula (I), wherein R1 is selected from the group consisting of: a) alkyl, alkenyl, alkaryl, alkcycloalkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl and heterocyclic; b) a substituted phenyl group of formula (II), wherein R is alkylene of from 1 to 8 carbon atoms, m is an integer equal to 0 or 1, and c) 1- or 2-naphthyl substituted at the 5, 6, 7 and/or 8 positions, R2 is selected from the group consisting of hydrogen, alkyl of from 1 to 4 carbon atoms, alkylalkoxy of from 1 to 4 carbon atoms, alkylthioalkoxy of from 1 to 4 carbon atoms; and R?3 and R3'¿ are independently selected from the group consisting of: (a) hydrogen, (b) alkyl, (c) -(R7)n(W)p, wherein R7 is an alkylene group, W is selected from the group consisting of (i) formula (A); (ii) heteroaryl; and (iii) N-heterocyclic, and n is an integer equal to 0 or 1, and p is an integer equal to 1 to 3; (d) -CH(ζ)CH¿2?C(O)O-Q where Q is selected from the group consisting of alkyl, aryl, heteroaryl and heterocyclic; X' is hydrogen, hydroxy or fluoro; X'' is hydrogen, hydroxy or fluoro, or X' and X'' together form an oxo group, Z is selected from the group consisting of a bond covalently linking R?1¿ to -CX'X''-, oxygen and sulfur.
WO2009048527A1 Substituted biphenyl gpr40 modulators The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
CN1618425A Composition contg. theaflavin and its derivatives, prepn. method and application thereof A composition for health-care food or beverage to prevent cancer, and cardiovascular and cerebrovascular diseases, or for medicine to treat cancer, AIDS and diabetes contains proportionally theaflavin or its derivative, phosphatide, cholesterol and assistant. Its preparing process is also disclosed.
WO2011140009A1 Methods of using semi-synthetic glycopeptides as antibacterial agents Methods of using semi-synthetic glycopeptides of formula I-XIV having antibacterial activity are described.
US20070299026 Immunosuppressive Cytokine The EB1-3-p35 cytokine is shown for the first time to be capable of inhibiting immune responses mediated or controlled by T cells via an effect on suppressor T cells. This suggests that EBI3-p35 may be therapeutically effective in a variety of inflammatory and autoimmune conditions including arthritis, atherosclerosis, allograft rejection, and allergies such as asthma.
EP2070928A1 7-azaindol-3-ylacrylamides active as kinase inhibitors Compounds represented by Formula (I) wherein R1 and R2 are as defined in the specification, compositions thereof, and methods of use thereof.
WO2009084982A1 Use of organic dyes as an agent for treating oncological diseases The invention relates to using organic dyes, the formula of which has a double bond N=N, the molecular mass ranges from 400 to 900 and which are selected from a group of Sudan dark blue, Congo red, Naphtol dark blue, Sudan IV, Bismarck brown, black acid and blue acid, as an agent for treating oncological diseases to be administered in the form of a single dose ranging from 0.1 mg to 2g up to three times a day. Mainly, the agentis used in the form of an aqueous solution or a physiological solution when diluted from 10-5 to 10-7 mmol/l. The aqueous solution is rectally administered or the 1-3% agent solution is intravenously injected, or the 1% agent solution is inhaled, or the agent-based 1-5% ointment is used or the agent is rectally administered in the form of suppositories. Thus, the invention discloses the effective medicinal agents which exhibit a wide spectrum of therapeutic modalities with respect to different oncological diseases and are devoid of side effects. Furthermore, the invention makes it possible to use effective, easily accessible, non-toxic substances, which are devoid of side effects when used in pharmaceutically acceptable doses, in the form of a therapeutic agent for treating oncological diseases, to reduce the length of treatment and to increase the effectiveness of treatment.
EP1572093A2 Improved treatment of cancer with glutamine Provided are methods of treating cancer, and/or the side effects of cancer therapy, involving the administration of glutamine, optionally in combination with a carbohydrate carrier that enhances the absorption of glutamine.
WO2011093811A2 Pharmaceutical preparations comprising formoterol and fluticasone The present invention relates to pharmaceutical compositions in dry powder form comprising formoterol and fluticasone and/or their pharmaceutically acceptable derivatives as active agents, and capsule and blister forms containing these pharmaceutical compositions so as to be used in treatment of respiratory tract diseases.
WO2008034644A3 Process for making anastrozole A process for making anastrozole using a 1-substituted triazole can reduce formation of the undesired iso-anastrozole. A typical process is represented by (I), wherein compound (10) is a 1-substituted triazole and compound (1) is anastrozole.
WO2009016253A2 Cyanomethyl substituted n-acyl tryptamines The present invention relates to cyanomethyl substituted N-acyl tryptamines of the formula (I) in which R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
EP1825852A1 ST104P as an anti-angiogenic agent The anti-angiogenic functions of a polysulfated, cyclic compound; ST104P, were investigated. ST104P exhibited excellent water solubility and low cytotoxicity to endothelial cells. ST104P potently inhibited the secretion of matrix metalloproteinase (MMPs) by endothelial cells. Moreover, ST104 also perturbed the migration and tube formation of endothelial cells. Application of ST 104P abolished the neovascularization in chicken choroiallantoic membrane (CAM) in a dose-dependent manner. Besides, repeated administration of ST104P into Lewis lung carcinoma resulted in delayed tumor growth and prolonged the life span of tumor-bearing mice. These results indicated that ST104P inhibited angiogenesis and may hold promises for treatment of cancer.
CN101310753A Analgesic and anticancer plaster and preparation method thereof The invention discloses an analgesic and anti-cancer plaster, which is prepared by raw materials such as pedate pinallia jackinthepulpit rhizome, common monkshood mother root, giant typhonium rhizome, frankincense, myrrh, long pepper, manchurian wildginger, dahurian angelica root, yanhusuo, pricklyash peel, pepper, aconitum brachypodum diels, edible tulip, toad venom, resina draconis, borneol, castor oil and litharge, etc. The analgesic and anti-cancer plaster has low cost, significant analgesic effect, exact efficacy, safety, no toxicity or side effects and very convenient usage. The invention further discloses a preparation method of the analgesic and anti-cancer plaster.
CN102178646A Stable Tegafur injection and preparation method thereof The invention discloses stable Tegafur injection and a preparation method thereof. The stable Tegafur injection is prepared mainly by the following steps of: mixing Tegafur and water for injection; adjusting the pH value to be 10.5 to 12.0 by using sodium hydroxide solution and/or acidic solution; adding an antioxidant and a pH value buffering agent and introducing nitrogen to perform protection; and performing high-temperature sterilization to prepare the injection. By the method, the Tegafur injection can be more stable; high-temperature sterilization can be performed; relative substances are greatly reduced compared with those in the prior art; particularly, the problems that the pH value is reduced, the color of the solution is changed to yellow, visible foreign matters are detected to be unqualified and relative substances are detected to be unqualified in the high-temperature sterilization and storage process of the Tegafur injection adopting the products in the prior art are solved; and the stable Tegafur injection can guarantee that the products meet the rule of the medicament quality standard and contributes to clinic administration and popularization.
WO2008105515A1 Novel hydroxamic acid derivative Disclosed is a novel compound which has a potent antibacterial activity on a gram-negative bacterium (e.g., Pseudomonas aeruginosa) or a drug-resistant mutant thereof relying on its and LpxC inhibitory activity, and which is therefore useful as a pharmaceutical agent. Specifically disclosed is a hydroxamic acid derivative represented by the general formula (1) below or a pharmaceutically acceptable salt thereof.
CN101337044A External preparation for mammary gland disease and preparation method thereof The invention relates to a preparation for external administration, which cures mammary diseases and comprises the following materials by weight ratio: 25 to 30 parts of rhizoma zedoariae, 20 to 30 parts of armand clematis, 40 to 50 parts of dandelion, 40 to 50 parts of bunge corydalis herb, 20 to 30 parts of fossil bone, 20 to 30 parts of oyster, 10 to 20 parts of mirabilite, 10 to 20 parts of bupleurum, 20 to 30 parts of Paris polyphylla, 20 to 30 parts of salvia miltiorrhiza, 20 to 30 parts of rhizoma corydalis, 20 to 30 parts of nutgrass galingale rhizome, 20 to 30 parts of motherwort, 20 to 30 parts of bitter orange, 5 to 15 parts of Clerodendron, and accessory materials. The preparation can be prepared into cream, ointment, lotion, liniment or emplastrum. The preparation method comprises the following steps: preparing the materials into the aqueous extracting solution, adding the substrate, stirring uniformly, filtering, adding spice, stirring and packaging. The preparation has the advantages of immediate effect, good curative effect, no gastrointestinal stimulation, no toxic or side effect, convenient administration, safety, reliability and long-term use, and is mainly applicable to cure and prevention of mammary diseases, such as hyperplasia of mammary glands, galactocele, etc.
EP2448938A1 Pyrimidinones as pi3k inhibitors The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
US20100048522 Ear infections, optionally with antiinflammatory agent Ophthalmic, otic and nasal compositions containing a new class of antibiotics (e.g., moxifloxacin) are disclosed. The compositions preferably also contain one or more anti-inflammatory agents. The compositions may be utilized to treat ophthalmic, otic and nasal conditions by topically applying the compositions to the affected tissues.
CN103690526A Antibacterial medicinal composition of azalomycin F derivative and vitamin K3 The invention discloses an antibacterial medicinal composition of azalomycin F derivative and vitamin K3. The antibacterial medicinal composition contains de-malonyl azalomycin F and vitamin K3. Experiments show that the de-malonyl azalomycin F and the vitamin K3 have a synergetic antibacterial effect, and the antibacterial activity of combination medication is improved by 4-8 times compared with that of separate medication; on the other hand, when the same antibacterial effect is achieved, the combination medication can ensure that the dose of each medication is reduced to be 0.125-0.25 times that of separate medication, so that the toxic or side effect of the separate medication is reduced. The experiments also show that the antibacterial medicinal composition consisting of the de-malonyl azalomycin F and the vitamin K3 has very good medicament development prospect and can be used for preparing a medicament for treating pathogen infection.
WO2010044371A1 Insulin secretion stimulator A sweet taste receptor agonist such as acesulfame K, sucralose, saccharin or glycyrrhizin can be used as an active ingredient for an insulin secretion stimulator. A candidate substance for an insulin secretion stimulator can be screened by: adding a compound to be tested to a cell in which a sweet taste receptor is expressed; measuring a sweet taste receptor signal; and selecting a substance that enhances the sweet taste receptor signal. The effect to stimulate the sweet-taste-receptor-mediated insulin secretion of a compound can be evaluated by: adding the compound to a cell in which a sweet taste receptor gene is expressed and a cell in which the expression of the sweet taste receptor gene is inhibited separately; and measuring the amount of insulin secreted in the cells separately.
EP1807434B1 Thienopyridines as allosteric potentiators of the m4 muscarinic receptor The present invention relates to selective allosteric potentiators of the Formula (I): or pharmaceutically acceptable salts thereof, for the treatment of disorders associated with M4 muscarinic receptors.
US20120277289 Activity generating delivery molecules Activity-generating delivery molecules comprising the structure R3—(C═O)-Xaa-NH—R4 wherein Xaa is any D- or L-amino acid residue with a non-hydrogen, substituted or unsubstituted side chain, R3—(C═O)— and —NH—R4 are independently a long chain group, each long chain group containing one or more carbon-carbon double bonds, and salts, compositions and methods of use thereof. The activity-generating delivery compounds and compositions are useful for generating activity of an active agent in a cell, tissue, or subject.
CN102895223A Dehydroandrographolide succinate compound-containing medicinal composition and its preparation method The invention provides a dehydroandrographolide succinate compound-containing medicinal composition and its preparation method. Being a freeze-dried powder injection, the medicinal composition provided in the invention comprises the following components: dehydroandrographolide succinate, mannitol, sorbitol and sodium bicarbonate, wherein the dehydroandrographolide succinate, the mannitol and the sorbitol are in a weight ratio of 100:3-20:1-10; and the pH value is 7.0-7.5. The dehydroandrographolide succinate freeze-dried powder injection provided in the invention has the characteristics of good stability, simple prescription, and less consumption of auxiliary materials.
US20110135629 EYA2S As Modifiers of the PTEN/AKT Pathway and Methods of Use Human MPTENAKT genes are identified as modulators of the PTEN/AKT pathway, and thus are therapeutic targets for disorders associated with defective PTEN/AKT function. Methods for identifying modulators of PTEN/AKT, comprising screening for agents that modulate the activity of MPTENAKT are provided.
US8193182 Substituted isoquinolin-1(2H)-ones, and methods of use thereof Chemical entities of Formula I: that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.
EP1656112A1 Buccal formulations of galanthamine and uses thereof Film-like medicaments for the buccal administration of galanthamine or of a salt or derivative thereof comprise at least one layer, which contains a centrally acting cholinergic active principle or a combination of at least two active principles of this type, whereby the active principle(s) is/are selected from the group consisting of galanthamine, pharmaceutically acceptable salts of galanthamine, galanthamine derivatives and the pharmaceutically acceptable salts thereof.
US20120164219 Peroral tablet for bowel cleansing To provide a peroral tablet for bowel cleansing which leaves no remains in the intestinal tract after bowel cleansing, which exhibits a dissolution property equivalent to that of conventional sodium phosphate-containing tablets including crystalline cellulose, and which is a small-size agent readily taken by a subject. The peroral tablet for bowel cleansing containing the following ingredients (A) and (B): (A) 80 to 95 mass % of sodium phosphate, and (B) (B1) 7 to 11 mass % of hydroxypropyl cellulose which has such a particle size that ≧99% of the particles thereof pass through a mesh having an opening of 350 μm and whose 2-mass % aqueous solution has a viscosity of 2.0 to 10.0 mPa·s, (B2) 5 to 13 mass % of hydroxypropyl cellulose which has such a particle size that ≧99% of the particles thereof pass through a mesh having an opening of 150 μm and whose 2-mass % aqueous solution has a viscosity of 3.0 to 5.9 mPa·s, or (B3) 7 to 11 mass % of hydroxypropyl cellulose which has such a particle size that ≧99% of the particles thereof pass through a mesh having an opening of 150 μm and whose 2-mass % aqueous solution has a viscosity of 6.0 to 4,000 mPa·s, and having a water-insoluble ingredient content of 5 mass % or less.
CN103211754A Production method of sterile stable pirenoxine sodium eye drops The invention discloses a production method of sterile stable pirenoxine sodium eye drops. The sterile stable pirenoxine sodium eye drops comprise a sterile solid drug packaged individually and a special-purpose solvent for dissolving the sterile solid drug. The sterile solid drug contains an active component and pharmaceutically acceptable auxiliary materials. The active component is pirenoxine sodium. According to the production method, the active component pirenoxine sodium and the pharmaceutically acceptable auxiliary materials are prepared into sterile freeze-dried powder and the sterile freeze-dried powder is dissolved in the special-purpose sterile solvent in clinical use. The production method can improve stability of the pirenoxine sodium eye drops, realize production of the sterile stable pirenoxine sodium eye drops, and improve safety of the sterile stable pirenoxine sodium eye drops in use.
CN1813760A Ceftiofur-containing powder injection for beast The present invention relates to a veterinary powder injection preparation containing ceftiofur for preventing and curing animal microbial infective diseases. It is characterized by that it contains 20-100% of ceftiofur free acid or ceftiofur hydrochloride aseptic powder, and the rest is medicinal auxiliary material. Besides, said invention also provides its application method.
US7838055 microcrystallization of xylitol and maltitol via spraying liquid feed thereof, evaporating solvent, conditioning, milling; for use in confectionery, foodstuffs, oral hygiene products and pharmaceuticals and dietetic The present invention relates to a microcrystallized polyol comprising at least two polyols, wherein said polyols are selected from the group consisting of maltitol, xylitol and lactitol and wherein said composition contains at least 25% by weight of each of at least two of said polyols microcrystallized together into a solid microcrystalline product. The present invention also relates to a process for the microcrystallization of polyols into a polyol composition. The microcrystallized polyol composition can be used in confectionery, foodstuffs, oral hygiene products and pharmaceuticals and in dietetic products.
US7576084 1-(Phenylmethylaminocarbonyl-),4,7-di(oxo-),6-(4-(hydroxylphenyl),8-(piperidino(1,3-phenylene)methyl)-perhydro(pyrazino(2,1-c)-as-triazine); disorders modulated by Wnt-signaling pathway; anticarcinogenic agents; colorectal cancer; restenosis; polycystic kidney disease; angiogenesis inhibition Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
CN1830430A Dichlofenas sodium slow release suppository and its preparation method A slow-release suppository of diclofenac sodium applied via rectum contains proportionally diclofenac sodium, matrix and carbomer.
US7384941 2-(phenoxymethyl)-and 2-(phenylthiomethyl)-morpholine derivatives for use as selective norepinephrine reuptake inhibitors Compounds of formula (I): wherein A is S or O; R is H; Ar is an optionally substituted phenyl group; X is an optionally substituted phenyl group, a C1-C4 alkyl, a C3-C6 cycloalkyl group or a CH2(C3-C6 cycloalkyl) group; R′ is H or C1-C4 alkyl; and each R1 is independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof are selective inhibitors of norepinephrine reuptake.
WO2007013677A1 Potentiator for substance having interferon-like effect Disclosed are a potentiator for the anti-hepatitis C virus activity of a substance having an IFN-like effect and an agent for alleviating an adverse side effect caused by a substance having an IFN-like effect. The potentiator or agent comprises at least one branched amino acid selected from isoleucine, leucine and valine or a salt thereof.
US20110009492 ß-PHENYLETHYLIDENEHYDRAZINE DERIVATIVES The present invention provides new β-phenylethylidenehydrazine derivatives, processes for preparing them and their use as pharmaceutical compostions. The β-phenylethylidenehydrazine derivatives according to the invention generally correspond to the general formula:
WO2011054875A1 Pharmaceuticals containing choline The invention relates to pharmaceuticals in particular for intravenous administration, containing choline or pharmaceutically acceptable salts or analogs thereof. The invention further relates to pharmaceuticals, in particular for intravenous administration, containing choline or pharmaceutically acceptable salts or analogs thereof, alone or in combination with vitamin C and/or L-arginine and/or vitamin D3 (cholecalciferol) for use in fighting CTCs, DTCs or inactive leukocyte precursors in the blood and bone marrow.
EP0907378B1 Method for the concentration of antibody solutions The present invention relates to a concentrated antibody preparation, pharmaceutical formulations containing such a preparation, its use in human therapy and processes for its preparation.
WO2011097788A1 Use of pentoxifylline for preventing or treating constipation Use of pentoxifylline in preparation of medicaments for preventing or treating constipation, a pharmaceutical composition comprising pentoxifylline for preventing or treating constipation and a method for treating constipation by using pentoxifylline are disclosed. The trial of the present invention proves that pentoxifylline can improve constipation, especially functional constipation.
CA2372384C Anti-inflammatory bioactive glass particulates Compositions and methods for systemically minimizing the inflammatory effects of TNF-.alpha. are disclosed. The compositions include particles of bioactive glass with a particle size less than about 20 µm, alone or in combination with anti-inflammatory agents and other therapeutic agents. The compositions can include an appropriate carrier for oral, intramuscular, intraperitoneal or intravenous administration. When administered to a patient, the particles bring about elevated levels of IL-6 and do not cause elevated levels of TNF-.alpha..
WO2006012310A3 Carbazole derivatives for treating polycystic kidney disease Compounds represented by Structural Formula (I): where X is -H, -OR, -SH, -OC(O)R, -OC(O)OR,-OC(O)NRR or -SC(O)OR have anti-cystogenic activity, particularly against polycystic kidney disease. Such compounds can be used in pharmaceutical compounds and in methods of treating polycystic kidney diseases. The invention also includes novel 3-hydroxymethyl-substituted carbazoles and compounds of Structural Formula (I) where Ring A is a 5-, 6-, 7- or 8- membered non-aromatic carbocyclic ring optionally substituted at one or more substitutable ring atoms.
WO2009073300A1 [1h- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase c-theta The present invention relates to compounds of formula (I) and (IA) useful as inhibitors of protein kinase (1a). The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. (a) : in particular protein kinase C theta, wherein A and A' are independently -N- or -C(R+) -. Ring B is five- or six-membered saturated carbocyclic or heterocyclic R1, R2, R3, R4, R5, R6, R7, x and y are as described herein.
US7414072 Aryl 5-thio-β-d-glucopyranoside derivatives and therapeutic agents for diabetes containing the same There is provided a 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.
US20100178323 Dermal Delivery Device A transdermal drug delivery device is disclosed. Over an extended wear period, the device causes cumulative moderate irritation plus significant irritation of less than 5% and/or achieves a meaningful degree of detachment over a seven day period of less than 20%.
US20100143492 Coagulation and fibrinolytic cascades modulator A thromboplastin reagent comprises (i) TF, (ii) a phospholipid, and (iii) a polyP TFPI blocker.
CN102614137B Gemcitabine hydrochloride freeze-dried powder injection and preparation method thereof The invention relates to a gemcitabine hydrochloride freeze-dried powder injection, which comprises the following substances in parts by weight: 100 parts of gemcitabine hydrochloride, 50-80 parts of mannitol, 1.5-2.5 parts of citric acid, 0.8-1.5 parts of sodium citrate and 10,000-25,000 parts of water for injection. The invention further relates to a gemcitabine hydrochloride freeze-dried powder injection and a preparation method thereof. The gemcitabine hydrochloride freeze-dried powder injection and the preparation method thereof related to the invention have the advantages that: (1) the stability is high: as proved by accelerated test, the main medicament content of the prepared gemcitabine hydrochloride freeze-dried powder injection does not change basically under an accelerated condition, the stability is higher, the contents of other relevant substances are lower and do not change remarkably, and the effect is remarkably superior to the prior art; (2) the safety is high: the conventional additive in the field of injections is adopted, so that the using amount is small, and the quality is controllable; and (3) industrial production is performed.
WO2006002840A3 Aerosol suspension formulations containing tg 227 ea or tg 134 a as a propellant The invention relates to propellant formulations containing at least one suspended active ingredient which contains chemically bound water, water, and the propellant TG 227 or TG 134 a.
US20100003262 Therapeutic, prophylactic and diagnostic agents for hepatitis b The present invention provides regulation of expression of toll-like receptors by the hepatitis B (HBV) pre-core protein, or its extracellular expression product the hepatitis B E antigen (HbeAg). Compounds regulating such expression have use in the treatment and prophylaxis of HBV infection in animal. The invention also provides methods for diagnosing HBV and agents useful in diagnostic protocols. The present invention further contemplates methods for monitoring disease states in humans and other animal species, including animal models, and providing an indication of the subject for infection by HBV, or development of other diseased states.
CN101260080A 3-(2-methyl-5-nitorimidazole)-1,2-propyl ester compound and its preparation method and use The invention discloses a novel nidazole ester compound, the chemical name of which is: 3-(2-methyl-5-nitroimidazol)-1, 2-acetoxypropane compound. The invention has a structure of general formula (I), wherein, R is selected from any one of CH3CO, OCCH2CH2COOH and SO3H. The compound has good anaerobic bacteria resistant effect and parasite resistant effect and so on, and has small side effect. The invention also discloses a preparation method and a use for the nidazole compound.
CA2845829A1 Compositions and methods for use in promoting lean body mass Food supplement compositions and their methods of use in promoting lean body mass are provided.
CA2213989C External preparation for topical administration The present invention is directed to an external preparation for topical administration which aims at inhibiting rejection reactions at organ diseases or allergic diseases and contains as the active ingredient 2-amino-2-(2-(4-octylphenyl)ethyl)propane-1,3--diol or a pharmaceutically acceptable acid addition salt thereof.
CN103243147A Novel high-throughput yeast cell-based screening platform for identifying HMG-CoA reductase inhibitors and uses of such inhibitors Methods of screening, identifying and isolating HMG-CoAR inhibitors are disclosed herein. In particular, said method is useful for screening natural raw products. The present invention also provides potent HMG-CoAR inhibitors for treatment and prevention of diseases and conditions associated with elevated cholesterol and/or blood lipid levels.
US8173133 Acyl pseudodipeptides which carry a functionalized auxiliary arm The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state. Compounds of the present invention have immunomodulating properties like adjuvants, In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targeting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.
EP1070067B1 Cytotoxic alkaloid derivatives including asmarine a and b isolated from a sponge Asmarine A and B, novel cytotoxic diterpene-alkaloids, have been isolated from the sponge Raspailia sp. The structure of these compounds have been established on the basis of NMR data and confirmed by X-ray analysis. Also claimed are compounds (I) or (II), wherein R1 represents hydrogen or lower alkyl or lower alkanoyl; R2 represents hydrogen or lower alkyl; R3 is either an alkyl or a cycloalkyl group containing one or more isopreneunits, or a monoterpene or a sesquiterpene or a sesquiterpene or a diterpene group; R4 or R5 represent hydrogen or lower alkyl; R6 represents lower alkyl; X represents F or Cl or Br or (I).
CN101642573B Chitosan-based hepatic-targeted nano-particle drug delivery system and preparation method thereof The invention relates to a chitosan-based hepatic-targeted nano-particle drug delivery system which takes a derivative of glycyrrhetinic acid-modified chitosan as a carrier material and is prepared by embedding an anti-cancer drug, the particle size of nano-particles is 50nm-300nm, and the drug-loading rate is 5-40%; and the carrier material is glycyrrhetinic acid-sulfate chitosan or glycyrrhetinic acid-carboxymethyl chitosan, and the embedded anti-cancer drug is doxorubicin, paclitaxel or hydroxycamptothecin. The chitosan-based hepatic-targeted nano-particle drug delivery system has the beneficial effects that the chitosan and the derivative thereof are non-toxic and have good biocompatibility and anti-tumor effect, the hepatic targeting tendency of glycyrrhetinic acid and excellent biological performance of the chitosan derivative are combined and a novel hepatic-targeted drug delivery system,is developed and prepared; and the hepatic-targeted nano-particle drug delivery system has drug sustained-release function and hepatic targeting property and can reduce the using amount of the drug and the administration times, reduce the toxicity or the side effects of the drug and improvethe efficacy by being used in the treatment of liver diseases, thereby having good application prospects.
EP1307445B1 Benzofuran derivatives and their use as antibacterial agents The invention relates to novel benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.
US20090035386 Conditioning of a patient's blood by gases The present invention relates to a method for using gas exchange modules for adjusting a pH value of blood in order to, e.g., adjust a non-physiological pH in patients treated with drugs whose activity optimum is in a non-physiological pH or to bring the pH to a physiological value.
US7125884 N-but-3-enyl norbuprenorphine and its use as analgesic The present invention provides compound having the structure: and pharmaceutically acceptable salts or derivatives thereof, as well as compositions including such compounds. The invention also provides methods of (1) preventing pain, (2) treating pain, (3) inducing sedation, (4) treating opiate addiction, (5) treating opiate withdrawal (abstinence syndrome) and/or (6) treating cough in a patient in need thereof by administering a compound or composition of the invention.
US7053105 Farnesyl transferase inhibiting quinoline and quinazoline derivatives as farnesyl transferase inhibitors This invention comprises the novel compounds of formula (I) wherein r, s, t, Y1—Y2, R1, R2, R3, R4, R5 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
CN102885911A Health protection medicine for exclusion of metal mercury The invention provides a health protection medicine for exclusion of metallic mercury, and belongs to technical field of health protection products. The present invention is mainly used for helping to exclude the toxic substance metal mercury which is known as lead by people out of the body. The composition of the present invention includes: mesona chinensis extract, ginseng extract, angelica sinensis extract, hawthorn extract, pseudo-ginseng extract, zinc lactate and licorice extract. The medicine enters a human body to release active substances which may be directly reacted with the metal mercury to form complexes to be excluded out of the body with urine or feces. The medicine is good in exclusion effect of metal mercury, non-toxic and harmless, and eventually reaches the health protection effect on the human body.
WO2014076170A1 Substituted pyrazolo[3,4-d]pyrimidine compounds, their preparation and use as|sigma receptors ligands The present invention relates to new substituted pyrazolo[3,4- d]pyrimidine compounds of general formula (I) having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them and to their use as medicaments for the treatment of i.a. pain. n is selected from 1, 2, 3 or 4; R1 represents a carbon-linked optionally substituted aryl or heteroaryl radical; R2 and R3 independently represent a hydrogen atom, an optionally substituted aliphatic, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl radical, or R2 and R3 together with the bridging nitrogen form an optionally substituted heterocycloalkyl or heteroaryl radical.
US20130065933 Pharmaceutical composition for peroral administration of diindolylmethane The invention relates to pharmacy. It comprises block copolymer pharmaceutical compositions containing 3,3′-diindolylmethane (DIM). The pharmaceutical composition for peroral administration comprises 3,3′-diindolylmethane as an active component and a target additive, the target additive being a block copolymer of oxyethylene and oxypropylene, in which the content of the hydrophobic block is less than 50 mass % and the molecular mass of the hydrophilic block is equal to 2,250 Da or more, at a ratio of the active component to the selected block copolymer varying between 10:1 and 2:1. The composition improves absorption of the active compound by the bloodstream upon peroral delivery.
CN101584712A Composite preparation composed of nervonic acid, composite mineral matter and composite vitamin The invention relates to a composite preparation composed of nervonic acid, composite mineral matter and composite vitamin, characterized in that, the composite preparation is made of raw materials based on the following weight percentage: 1-90 % of nervonic acid, 1-80 % of composite mineral matter, 1-80 % of composite vitamin, and 1-50 % of granular formulation, tablet and capsule excipient to make into granular formulation, capsule and tablet. The nervonic acid, mineral matter and vitamin required by human body can be provided.
WO2008096730A1 Anti-inflammatory agent and use thereof Disclosed are: a novel anti-inflammatory agent; and use of the anti-inflammatory agent. Specifically disclose is an anti-inflammatory agent comprising acetic acid or a salt thereof as the main component. The anti-inflammatory agent can exhibit its anti-inflammatory effect through the specific inhibition of the activation of a transcription factor NFAT. When the anti-inflammatory agent is used in combination with a steroidal anti-inflammatory agent, a higher therapeutic effect can be produced.
WO2008015942A1 Therapeutic agent for neuroblastoma, method for screening for the therapeutic agent, and method for determination of prognosis of neuroblastoma A method for screening for a therapeutic agent for neuroblastoma, comprising the steps of: culturing a cell in the presence or absence of a compound to be tested; measuring the expression level of a Shf gene in a cultured cell; and determining the compound as being a therapeutic agent for neuroblastoma when the expression level of the Shf gene in a cell cultured in the presence of the compound is higher than that in a cell cultured in the absence of the compound.
US7910739 tacrine derivatives such as N-[5(6-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamino)pentyl]-3-(1H-indol-3-yl) propionamide, used for treatment of neurodegenerative diseases; bioassays The invention provides compounds of formula: which have a tacrine moiety connected to an heterocyclic moiety through a linker. Through careful selection of the substituents and the linker, the activity and selectivity towards acetylcholinesterase can be modulated. The compounds show potent AChE inhibition activities together with modifications in the β-amyloid aggregation properties by binding simultaneously to the catalytic and peripheral AChE sites. They are useful in the treatment of AChE mediated diseases, such as the Alzheimer's disease.
EP1251824B1 Use of a beverage composition comprising a polyphosphate for treating dental erosion The present invention is directed to a method of treating dental erosion comprising orally administering to a mammal (preferably, a human) a beverage composition having a pH of less than about 5; wherein the beverage composition comprises a compound having the structure (I), wherein n is an integer averaging from about 7 to about 100 and M, M' and M'' are each, independently, selected from the group consisting of sodium and potassium. The present invention is further directed to kits comprising the foregoing beverage composition and information that use of the beverage composition provides treatment against dental erosion.
US20120122831 Method and device for rapid detection of bacterial antibiotic resistance/susceptibility Described herein is a method and a device for expediting delivery of an agent to a damaged bacterial cell. In one embodiment, the methods and devices are useful for screening candidate antibiotics. In another embodiment, the methods and devices described herein are used to determine susceptibility of bacteria to an antibiotic. The methods also provide a method for determining an appropriate antibiotic to treat an individual having a bacterial infection.
CN101260073A Quasi-peptides HIV-1 protease inhibitor, preparation method and use The invention discloses a new inhibitor, a preparation method and a use for peptidomimetic HIV-1prolease. In a formula (I) compound, R1 represents phthalimide radical, 2-methoxyphenoxyl, 4-methoxyphenoxyl, 2, 6-dimethylphenoxyl, 2-nitrylphenoxyl, 4-nitrylphenoxyl, indole-3-methylene, saccharin radical and 2-benzoxazol, R2 represents hydrogen, linear chain or branched chain (C1-C4) alkyl, -CH2OH and =CH2, and R3 represents 2-naphthyl, 2(3H)-benzoxazol-6-radical.
CN102153538B Benzocyclodirivative The invention belongs to the technical field of medicaments, in particular relates to a benzocyclodirivative as shown in a general formula (I) as well as pharmaceutically acceptable salts, a hydras and an isomer thereof, wherein R1, R2, R3, R4, Q, X and Y are defined in the specification. The invention also relates to a preparation method of the compounds, a pharmaceutical composition containing the compounds and application of the compounds in preparing medicaments for treating and/or preventing non-insulin-dependent diabetes mellitus.
US20100298419 Antibiotic-free plasmid The present invention provides a method of maintaining a gram negative bacterium plasmid without the use of antibiotic selection pressure. Further, the invention relates to the drugless plasmids produced including drugless plasmids containing a heterologous gene. The invention also provides formulations and/or compositions comprising the drugless plasmids comprising a heterologous gene, formulations and/or compositions comprising a protein or an immunogen expressed using the drugless plasmids, and methods of administering such formulations and/or compositions to a host. The invention relates to gram negative bacteria containing the drugless plasmids.
WO2009138516A1 Therapy regimen for treating acne related diseases The present invention relates to a novel therapy regimen for the treatment of acne related diseases. The novel therapy regimen adds a topical fixed-dose combination of a retinoid and an anti-bacterial agent, such as BPO, to a course of oral antibiotic therapy.
US20060142290 Compositions for affecting weight loss Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity.
CN103251550A Transdermal delivery ointment containing colchicine, and preparation method thereof The invention provides a transdermal delivery ointment. The transdermal delivery ointment comprises 0.05-10wt% of colchicine, 5-45wt% of medical sterile water, 5-30wt% of a water-soluble excipient, 10-60wt% of an oil-soluble excipient, and 0.1-10wt% of a transdermal enhancer, wherein the sum of the percentages of the above components is 100wt%. The invention also relates to a preparation method of the transdermal delivery ointment. The transdermal delivery ointment can be directly used against foci, and can avoid the generation of side effects of colchicine.
WO2008047948A1 Block copolymer for drug complex and pharmaceutical composition Disclosed is a block copolymer for a drug complex, which comprises a water-soluble polymeric segment comprising a polyethylene glycol and a polyamino acid segment having a hydrazide group and a hydrophobic group in a side chain.
US20120238584 5-HT1A receptor subtype agonist The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1) wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.
US7332504 Heterocyclic substituted aminoazacycles useful as central nervous system agents Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
WO2014100881A1 Compounds, use, reductase-inhibiting pharmaceutical composition in microorganisms, inha binder and method for obtaining inha binders The present invention describes novel and inventive enzymatic inhibiting compounds in microorganisms. In a preferred embodiment, the compounds of the present invention are used to inhibit the 2-trans-enoyl-ACP (CoA) reductase enzyme in microorganisms.
US20090176706 Materials and methods for treatment of inflammatory and cell proliferation disorders The present invention pertains to methods for treatment of inflammatory and cell proliferation disorders, such as cancer, by administering an agent that reduces atrial natriuretic peptide receptor-A (NPR-A) activity. In one aspect, the invention concerns a method for treatment of inflammatory and cell proliferation disorders, such as cancer, by administration of an effective amount of natriuretic hormone peptide (NP), or a polynucleotide encoding NP and an operably-linked promoter sequence. In another aspect, the present invention includes a pharmaceutical composition comprising an agent that reduces the activity of atrial natriuretic peptide receptor-A (NPR-A), and an anti-cancer agent. In another aspect, the present invention further concerns a method for identifying an agent useful for treating an inflammatory or cell proliferation disorder, comprising determining whether the agent reduces the activity of atrial natriuretic peptide receptor-A (NPR-A).
EP1225174B2 Anhydrous mirtazapine crystals and process for the production thereof Lowly hygroscopic anhydrous mirtazapine crystals exhibiting a moisture absorption of as low as 0.6 wt. % or below as stored for 500 hours in the air under the conditions of 25 °C, relative humidity of 75 %, and atmospheric pressure; a process for the production thereof; crystals of mirtazapine hydrates represented by formula (I); and a process for the production thereof (wherein n is an integer of 1 to 5). According to the process, stable anhydrous mirtazapine crystals little exhibiting hygroscopicity can be produced by simple industrial means, and the obtained anhydrous mirtazapine crystals are suitably usable as antidepressant by virtue of their extremely low hygroscopicity.
US20070243266 N-[1(R)-(3H-imidazo[4,5-b]pyridin-2-yl)ethyl]-2-fluoro-4-methyl-3-oxo-4-aza-5 alpha -androst-1-en-17 beta -carboxamide; osteoporosis, periodontal disease, bone fracture, frailty, sarcopenia, depression, sexual dysfunction, and cognitive decline; tissue-selective androgen receptor modulators(SARM) Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
CN101084895A Staphylococcus tryptophanyl-tRNA synthetase inhibitor The invention belongs to biological technique field, relates to small molecular inhibitor against staphylococci tryptophanyl-tRNA synthetase (WRS), molecular structure of the inhibitor shown in formula I, method of the inhibitor as medicament for preventive or treating relevant bacterial disease. Biochemical and biological experiments have shown that the inhibitor has strong binding force with target protein staphylococcus epidermidis or Staphylococcus aureus tryptophanyl-tRNA synthetase, can inhibit the activity of the synthetase, inhibit the growth of staphylococcus epidermidis Staphylococcus aureus. It has no toxicity to mammalian cell. The inventive inhibitor can be used for preparing medicament for treating disease caused by staphylococci, and preparing into disinfectant liquid.
WO2012065963A3 Antiviral condensed heterocyclic compounds The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting 5 properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection.
US8334263 Analgesic methods and compositions Compositions of flupirtine for management of neuropathic or inflammatory pain optionally including one or more other analgesics including opiates, NSAIDS and other active agents in immediate and controlled release forms. Methods and systems for administration of these compositions.
WO2009052708A1 1-(3-amino-propyl)-piperidin-4-yl-amides, pharmaceutical compositions, processes for their preparation and uses 1-(3-Amino-propyl)-piperidin-4-yl-amides as the following formula, pharmaceutically acceptable salts thereof , compositions thereof, and processes for preparing them. These compounds or their pharmaceutically acceptable salts could be used as antagonists of CCR5, are used to prepare drugs for treatment of CCR5 mediated diseases or HIV infection, asthma, rheumatoidarthritis, autoimmune diseases, chronic obstructive pulmonary disease(COPD).
CN101007011B Ginsenoside Rh2 self-emulsifying composition and its preparation method The invention has provided a micro emulsion compound which contains panaxoside Rh2, the panaxoside Rh2 and micro emulsion system is included in the invention. The mentioned micro emulsion system includes oil phase, surface acting agent and accessory surface acting agent. The compound in the invention can be used in the application and industrial production of liquid capsule, solid capsule, capsulae enterosolubilis or micro emulsion pellets based on solid support. The preparing method of the compound is also included in the invention. After being orally taken, the preparation can form O/W micro emulsion the diameter of which is smaller than 100nm. Since the medicine is dispersed in the micro emulsion, it can increase the releasing amount of the medicine and the stability is also increased;the oral bioavailability is 5-6 times of common preparations.
US20100179112 Nutritional Intervention for Improving Muscular Function and Strength The present invention provides a composition comprising HMB and Vitamin D. Methods of administering HMB and Vitamin D to an animal are also described. Vitamin D and HMB are administered to increase muscle mass, strength, and functionality. The combination of Vitamin D and HMB together has a synergistic effect, which results in a surprising and unexpected level of improvement in muscle mass, strength and functionality.
CN103539793A Thiazole carboxamide compounds and application thereof The invention provides thiazole carboxamide compounds with an effect of treating and/or preventing tumors, and a preparation method thereof, as well as pharmaceutically acceptable salts, solvates, chemical protection forms and prodrugs of the compounds.
CA2534496A1 Pyrimidylpyrrole derivatives active as kinase inhibitors Pyrimidylpyrrole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
WO2010054565A1 The water-soluble prodrug of (r)-(-)-bicalutamide, its preparation method and uses thereof The present invention provides the water-soluble prodrug of (R)-(-)-bicalutamide as follows of formula (I), its pharmaceutically acceptable salts, its preparation method and uses thereof. The compound of formula (I) is useful for treatment prostate cancer of male or man and the diseases associated with androgens.
WO2013177053A1 Pyrimidino [1, 2 -c] quinazolinone derivatives as tyrosine kinases inhibitors The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein variables R, Ar, X, and Ar1 and n are as defined herein. The compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
WO2006080312A1 Method for producing adsorptive porous body Disclosed is a method for producing a 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H- pyridazin-3-one adsorptive porous body which is characterized in that a porous body is processed with a halogen-containing organic solvent in which 2-benzyl-5-(4-chlorophenyl)-6- [4-(methylthio)phenyl]-2H-pyridazin-3-one is dissolved. This method is simple and easy, and the thus-obtained adsorptive porous body is excellent in properties of dissolving 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H- pyridazin-3-one out therefrom.
US7214690 For therapy of acne, male- pattern baldness, sexual dysfunction, impotence, wasting diseases, hirsutism, hypogonadism, prostatic hyperplasia, osteoporosis, cancer cachexia, and hormone-dependent cancers Novel non-steroidal tricyclic quinolinone and tricyclic quinoline compounds and compositions that are agonists, partial agonists and/or antagonists for androgen receptors (AR), their preparation and their uses are described.
WO2014038873A1 COMPOSITION FOR INHIBITING CELLULAR SENESCENCE COMPRISING QUERCETIN-3-O-β-D-GLUCURONIDE The present invention relates to a composition for inhibiting cellular senescence comprising quercetin-3-O-β-D-glucuronide (Q3GA) as an active ingredient, and provides a composition for inhibiting cellular senescence of fibroblasts or umbilical vein endothelial cells induced by adriamycin or replicative senescence of fibroblasts or umbilical vein endothelial cells. Specifically, the quercetin-3-O-β-D-glucuronide (Q3GA) is characterized by being isolated from Polygoni avicularis herba extract. The composition may be usefully used for treating aging-related diseases, for example, skin aging, rheumatoid arthritis, osteoarthritis, hepatitis, chronically damaged skin tissue, arteriosclerosis, prostatic hyperplasia and liver cancer, by inhibiting a cellular senescence process of human fibroblasts and umbilical vein endothelial cells.
CN101829328A Drug for treating amphetamine-type exhilarant dependence syndrome and amphetamine-type exhilarant and opioid mixed dependence syndrome The invention relates to a drug for treating amphetamine-type exhilarant dependence syndrome and amphetamine-type exhilarant and opioid mixed dependence syndrome, which comprises the following components in percent by weight: 2-95 percent of antipsychotics, 0.001-5 percent of a2 adrenergic receptor agonist, 0-5 percent of anticholinergic drug, 0-80 percent of non-opiates pain easing agent and 0-10 percent of benzodiazepines drugs. When used for treating symptoms occurring in patients abusing exhilarants of Benzedrine and the like or integrally abusing opioid, the drug achieves better effect, can rapidly and remarkably control abstinence syndrome, and has detoxification cure rate reaching over 90 percent.
US8088827 Use of irbesartan for the preparation of medicinal products that are useful for treating pulmonary hypertension The present invention relates to the use of irbesartan for the preparation of medicinal products that are useful for preventing or treating pulmonary arterial hypertension or pulmonary hypertension.
WO2009031922A1 Tablet for prophylaxis and treatment of dental and periodontium diseases The invention relates to stomatology and specifically to tablet for prophylaxis and treatment of dental and periodontium diseases. The tablet contains following components at a ratio, wt %: Magnesium sulfate or magnesium chloride or magnesium lactate or magnesium oxalate: 3.26-5.26, Pyridoxine hydrochloride: 0.060-0.074, Thiamin mononitrate: 0.50-0.062, Calcium glycerophosphate: 30.0-38.9, Ground laminaria thallus or dried laminaria aqueous extract: 1.1-2.2, Stevioside: 0.3-0.9, Sorbite: 10.0-25.0, Xylite: 10.0-25.0, Auxiliary components: 15.62-45.42
CN102670564A Preparation method for nimodipine sustained-release pellet capsule The invention belongs to the field of pharmacy and relates to a medicinal preparation and a preparation method thereof, in particular to a nimodipine sustained-release pellet capsule and a preparation method thereof. The nimodipine sustained-release pellet capsule comprises an active ingredient, auxiliary materials, fillers, a binder, solubilizing agents, lubricating agents and coating agents, wherein the active ingredient is nimodipine; the fillers comprise lactose, microcrystalline cellulose, starch, mannitol and powdered sugar; the binder is hydroxypropyl methylcellulose; the solubilizing agents comprise polysorbate-80 and poloxamer 188; the lubricating agents comprise polyethylene glycol 6000 and magnesium stearate; and the coating agents comprise polyvinyl alcohol coating powder and ethylcellulose coating powder.
WO2013110796A1 Thiazolidinedione derivatives, preparation thereof and use thereof in cancer treatment The present invention relates to thiazolidinedione derivatives, to the processes for preparing same and to the therapeutic use thereof for preventing or treating cancer, and more specifically breast cancer. These compounds are of formula (I) and exhibit, at a concentration of 100 µM, a hepatocyte viability preferably greater than 60%, preferably greater than 80% and more preferentially greater than 85%.
WO2013106646A2 Compounds and methods for the inhibition of vcb e3 ubiquitin ligase The present invention relates to novel compounds which find utility as modulators, especially inhibitors of VCB E3 Ubiquitin Ligase and as bioactive agents for use as therapeutics for the stimulation of erythropoiesis in a patient or subject including inducement of EPO production in the patient or subject, for the treatment of chronic anemia and ischemia (limits brain injury during episodes of localized anemia, ischemia and/or stroke and damage to cardiovascular tissue during cardiovascular ischemia), as well as enhancing wound healing processes. Pharmaceutical compositions comprising effective amounts of compounds according to the present invention alone or in combination with an additional erythropoieses stimulating agent such as EPO under the tradename procrit or epogen or darbapoietin alfa under the tradename aranesp. Methods of stimulating erythropoiesis in a subject or patient, including increasing the number of red blood cells and/or hematocrit of the patient, treating anemia, including chronic anemia and anemia associated with chronic kidney disease, dialysis, and cancer chemotherapy, ischemia, stroke and damage to cardiovascular tissue during cardiovascular ischemia as well as enhancing wound healing processes and preventing/reducing scarring secondary to healing represent additional aspects of the present invention. Local enhancement of angiogenesis through induction of VEGF including wound healing and reduction of stent occlusion remain additional aspects of the present invention.
EP2291353A1 Therapeutic prostaglandin compounds used as ocular hypotensive agents Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed, wherein a dashed line represents the presence or absence of a bond; and, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.
EP1891959A1 Contraceptive compositions for decrease risk of inborn errors Pharmaceutical composition (I) for contraception and to reduce the risk of congenital malformations comprises a daily dose of 2 mg or 1.5 mg of 17alpha -cyanomethyl-17-beta -hydroxyestra-4,9-diene-3-one (dienogest), 0.015 mg of 17 alpha -ethinylestradiol (ethinylestradiol) and (6S)-5-methyl-tetrahydrofolate, together with pharmaceutical acceptable auxiliary agents/carriers. An independent claim is included for a kit comprising 21 daily dose unit of (I) and 7 daily dose unit of (6S)-5-methylhydrofolate. - ACTIVITY : Contraceptive; Cardiant; Antimicrobial; Uropathic; Cytostatic; CNS-Gen. - MECHANISM OF ACTION : None given.
US20120270820 Use of albiflorin for anti-depression A pharmaceutical composition containing albiflorin and use thereof in manufacturing medicaments for preventing and treating depression are provided by the present invention.
CN102552259A Iloperidone inclusion compound included by beta-cyclodextrin and medicinal composition thereof The invention relates to an iloperidone inclusion compound included by beta-cyclodextrin or a derivative thereof. The inclusion compound which can substantially improve the solubility of iloperidone in water can be conveniently prepared into various compositions or preparations, especially injections. The injections can reduce the stimulation of iloperidone to intramuscular injection parts. The inclusion compound or the composition preparations thereof can be used for treating schizophrenia.
WO2003061362A3 Methods and compositions for treating polycystic ovary syndrome The present invention relates to methods of treating polycystic ovary syndrome (PCOS) comprising administering glucagon-like peptide-1 (GLP-1) to subjects suffering therefrom.
CN102671091A Medicine composition for preventing surgical postoperative uroschesis The invention discloses a medicine composition for preventing surgical postoperative uroschesis. The medicine composition is characterized in that raw material medicine consists of aralis tengyuch euonymus bark, cowherb seed, resurrection lily rhizome, saponin, fistular onion stalk, almond, mother chrysanthemum, elecampane, borneol and peach gum. Clinical study results show that the medicine composition can reduce the occurrence rate of the surgical postoperative uroschesis, the urination condition of patients is effectively relieved, the safety performance is good, the operation is simple and convenient, the painlessness is realized, and the medicine composition can be easily accepted by patients.
CA2264941C Use of a combination of an atypical antipsychotic and a serotonin reuptake inhibitor for treatment of psychosis The invention provides pharmaceutical compositions which comprise a first component which is an atypical anti-psychotic in combination with a second component which is a serotonin reuptake inhibitor, use of such compositions for treating a patient suffering from or susceptible to psychosis, acute mania, mild anxiety states, or depression in combination with psychotic episodes, and particularly such compositions which comprise a first component which is olanzapine and a second component which is fluoxetine hydrochloride.
EP1892299A2 Sense mRNA therapy Eukaryotic mRNA that encodes a protein of therapeutic interest is stabilised by at least one chemical modification. The stabilisation of the mRNA permits its use in sense RNA therapy wherein therapeutic proteins of interest are expressed transiently in cells. Modifications include 3' blocking, 5' blocking, a modified diguanosine (m7) cap linked to the mRNA by a chemically modified linkage, a 2' modified oligonucleotide, a poly A tail of greater than 50 bases in length, or a phosphorothiorate modification. Various disease states may be treated using such modified sense RNAs expressing relevant therapeutic proteins, including cystic fibrosis; muscular dystrophy; sickle cell anemia; thalasemia, coronary arterary disease, cancer, inflammation, stroke, heart disease, thrombosis, anemia, spinal-muscular atrophy, epilepsey, wound healing, septic shock, asthma, viral infection, bacterial or parasitic infection, diabetes, metabolic diseases, urea cycle disorders, Gaucher, schizophrenia, depression, Parkinson's disease, renal failure, liver failure, arthritis, impotence, baldness, pain, ulceration, and enlarged prostate.
US20080306048 Therapeutic pyrazoloquinoline urea derivatives The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
CN101578094A Robust sustained release formulations of oxymorphone and methods of use thereof Robust sustained release formulations, solid dosage forms comprising robust sustained release formulations, and methods for making and using these formulations and solid dosage forms are provided. Robustness of the sustained release formulation is related to the particle size of the hydrophilic gum. Sustained release formulations resist dose-dumping when ingested with alcohol. The formulations are useful for treating a patient suffering from a condition, e.g., pain. The formulations comprise at least one drug. In one embodiment, the drug is an opioid, e.g., oxymorphone.
WO2014128585A1 Azabenzimidazole compounds as inhibitors of pde4 isozymes for the treatment of cns and other disorders The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined 5 herein. The compounds of formula I are useful as inhibitors of PDE4 for the treatment of CNS and other disorders.
CN1823836A Medicine and food dual purpose nutritive product for preventing and treating pseudomyopia and its manufacturing method A Western medicine used as both medicine and food for preventing and treating pseudomyopia is prepared from vitamins, trace elements and minerals. Its preparing process is also disclosed.
US20090170765 Peptide for inhibition of calcineurin The present invention relates to a method for diagnosing susceptibility for a myocardial and/or immunological disorder, a kit and a therapeutic agent comprising a peptide of SEQ ID NO: 1 or 2 and uses thereof.
EP1461308B1 Bacterial enzyme inhibitors Compounds of formula (I), are antibacterial agents, wherein: Z represents a radical of formula -N(OH)CH(=O) or of formula -C(=O)NH(OH); X represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical; n is O or 1; and R represents an optionally substituted carbocyclic or heterocyclic group.
CN102070658A Dimer salt of steroid alkaloid and preparation and application thereof The invention discloses a dimer salt of steroid alkaloid, namely a dimer salt of 3-sec-butyl-4-methyl-2,3-dihydro-1H-pyrrolo-(3,4-b) quinoline-1,9(4H)-diketone. A preparation method for the dimer salt of the steroid alkaloid comprises the following steps of: culturing marine-derived fungus Penicillium sp.CCTCC No:M2010088 by using an artificial seawater GYT medium to obtain a strain, and extracting by using methanol to prepare an extract; performing column chromatographic separation by using 200-300-mesh column chromatography silica gel; performing gradient elution by using chloroform and methanol in a volume ratio of (10-0):1, and collecting components of which the Rf is 0.5; and recrystallizing by using methanol to obtain the dimer salt of the steroid alkaloid. The dimer salt of the steroid alkaloid has obvious anti-tumor effect, has the half inhibiting concentration of 19.38+/-0.15mu g/ml for human lung cancer cells in vitro, and may be a potential anti-tumor medicine.
CN101596158A Compound slow release preparation of acetyl aminophenol, pseudoephedrine and dextromethorphan The invention relates to a slow release preparation taking acetyl aminophenol, pseudoephedrine or physiologically acceptable slat thereof and dextromethorphan or physiologically acceptable slat thereof as active ingredients. The slow release preparation is characterized in that a releasing system comprises a tablet core and/or pill core capable of enabling a medicament to slowly release and a coating, wherein one part and/or all of the active ingredients exist in the tablet core and/or pill core, and the rest of the active ingredients exist in the coating.
US7863269 Imino-imidazo-pyridine derivatives having antithrombotic activity The invention relates to compounds of the formula I having antithrombotic activity, which in particular inhibit the protease-activated receptor 1 (PAR1), processes for their preparation and use thereof as medicaments.
DE102009011742A1 Aqueous liquid formulation, useful for treating migraine, comprises phospholipids, coenzyme Q10, blueberry extract (extract of Vaccinium myrtillus), and polyol comprising e.g. aldose, ketose, reduced aldose and/or ketose Aqueous liquid formulation (I) comprises: one or more phospholipids (a) (0.1-30 wt.%); coenzyme Q10 and/or its derivatives (b) (0.05-20 wt.%); blueberry extract (extract of Vaccinium myrtillus) (c) (1-20 wt.%); and one or more polyols (d) (5-90 wt.%) comprising aldose, ketose, reduced aldose and/or ketose, glycosides of aldoses and/or ketoses, 3-6C-tri, -tetra-, -penta- or -hexa-ol. Independent claims are included for: (1) a solid material obtained from the formulation by drying, preferably spray drying or freeze drying; and (2) a pharmaceutical preparation comprising (I) or a solid material. - ACTIVITY : Antimigraine. - MECHANISM OF ACTION : None given.
CN1721428A Compound and method for treating cancer The present invention provides is the compound and method of lowering SLP-2 expression or inhibiting SLP-2 protein activity to treat cancer. Specifically, the present invention discloses antisense oligonucleotide, nucleic acid, antibody, oligonucleotide adaptor, their arbitrary combination, or medicine containing them capable of lowering SLP-2 expression. The present invention also discloses method of detecting cancer and screening anticancer medicine. The said cancer is preferably high SLP-2 expression cancers, especially esophagus squamous carcinoma, endometium cancer and/or lung cancer.
US20090105221 Muscarinic receptor antagonists This present invention generally relates to muscarinic receptor antagonists of Formula (I), which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the prepration of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.
CN103751129A Secnidazole tablet with improved solubility The invention provides a secnidazole tablet with improved solubility. Polyvinyl pyrrolidone, pregelatinized starch, microcrystalline cellulose, alginic acid and sodium carboxymethyl starch are used as disintegrating agents. The secnidazole tablet comprises 20-45% of a filler, disintegrating agents, an adhesive and a lubricant. The filler is selected from lactose, cane sugar, glucose, mannitol, sorbitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, starch, carboxy methyl starch, pregelatinized starch, microcrystalline cellulose and dextrin. The secnidazole tablet with improved solubility provided by the invention can rapidly disintegrate and fully dissolve, so as to ensure the full play of treatment effect of the drug.
US20110092577 Inositol Pyrophosphates Determine Exocytotic Capacity The invention provides reagents and methods for treating type II diabetes, as well as methods for identifying compounds for treating type II diabetes.
US20120252825 Beneficial effects of combination therapy on cholesterol The present invention discloses pharmaceutical combination therapies for the treatment or prevention of diseases in a mammal comprising a Janus Kinase inhibitor or a pharmaceutically acceptable salt thereof and a HMG-CoA reductase inhibitor or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions containing the same and kits for achieving a therapeutic effect in a mammal comprising pharmaceutical combination therapies are further described.
CN101502647B Medicament composition for preventing or/and treating decayed tooth and preparation method thereof The invention provides a medicine combination for preventing and controlling or/and treating decayed teeth, which is prepared by taking dextran enzyme and sodium fluoride as active ingredients; wherein, each milliliter of the medicine combination contains 10-80mug of NaF and 1-4U of dextran enzyme. The invention also provides a preparation method of the medicine combination; the medicine of the invention jointly employs the sodium fluoride with a dosage lower than clinical dosage and Dex to reduce the use amount of the former; the medicine on Sub-MIC thereof can play a role in inhibiting dental plaque biomembrane and effectively increase anticarious effect of fluoride, and decrease toxic side effect thereof, control the biomembrane in light of control of exopolysaccharide and provide experimental basis and clinical choice for improving the healing effect of the medicine while reducing toxicity of the fluoride.
WO2006134613A3 Novel 5-substituted indole derivatives as dipeptidyl peptidase iv (dpp-iv) inhibitors The present invention relates to 5-substituted indole derivatives of formula (I): having inhibitory potential of dipeptidyl peptidase IV (DPP IV) enzyme where x and R1 are defined as defined in the specification
WO2013160642A3 Wound treatment The present invention concerns an isolated polynucleotide comprising a nucleotide sequence having substantial homology to any of the following nucleotide sequences: catcgttatgggacta, cattcttgatccttcc, cttttcaatctgactg, atgaaaatactcataa, gtgataaaagaaccat, gggttcatgaaagtga, gatgaccctcttatcc, tggaaggaatgtctgg, gcatctgcttccaaca, catcgttaggctagctacaacgatgggacta, tccaccaaggctagctacaacgaccatcaaa, gtcaacaaggctagctacaacgatgagctca, and cttttcaaggctagctacaacgactgactgt, and their use in the treatment of wounds.
CN102718730A Methods of synthesis and/or purification of diaminophenothiazinium compounds This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesis and/or purification of certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as ''diaminophenothiazinium compounds'') including Methylthioninium Chloride (MTC) (also known as Methylene Blue). The present invention also pertains to the resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment, prophylaxis, and diagnosis, etc., for example, a tauopathy; a disease of tau protein aggregation; Alzheimer's disease (AD); Pick's disease; Progressive Supranuclear Palsy (PSP); fronto temporal dementia (FTD); parkinsonism linked to chromosome 17 (FTDP-17); disinhibition-dementia-parkinsonism-amyotrophy complex (DDPAC); pallido-ponto-nigral degeneration (PPND); Guam-ALS syndrome; pallido-nigro-luysian degeneration (PNLD); cortico-basal degeneration (CBD); mild cognitive impairment (MCI); skin cancer; melanoma; methemoglobinemia; a viral infection; a bacterial infection; a protozoal infection; a parasitic infection; malaria; visceral leishmaniasis; African sleeping sickness; toxoplasmosis; giardiasis; Chagas' disease; Hepatitis C virus (HCV) infection; human immunodeficiency virus (HIV) infection; West Nile virus (WNV) infection; a synucleinopathy; Parkinson's disease (PD); dementia with Lewy bodies (DLB); multiple system atrophy (MSA); drug-induced parkinsonism; and pure autonomic failure (PAF).
US8642584 Method of using PI3K and MEK modulators The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
WO2011128434A2 Treatment of endocrine resistant breast cancer The invention relates to pyrimidylaminobenzamides of formula (I) and other suitable PDGF-R inhibitors, alone or in combination with at least one aromatase inhibitor for the treatment of endocrine resistant breast cancer and to a method of treating warm-blooded animals including humans suffering from endocrine resistant breast cancer by administering to a said animal in need of such treatment an effective dose of a pyrimidylaminobenzamide of formula I alone or in combination with an aromatase inhibitor.
US20080292553 Phosphoramidate Derivatives of Fau The present invention provides phosphoramidate derivatives of a furanosyluracil analog, FAU, that can effectively deliver FAU monophosphate, or a derivative thereof, intracellularly. FAU-Phosphoramidate diesters can bypass the first step of phosphorylation and be activated intracellularly so as to be converted to nucleoside monophosphates. This results in improved formation of nucleoside triphosphates, and higher incorporation into DNA. The compounds of the invention can be used to treat cancer.
US20110082202 Fatty acid acifran derivatives and their uses The invention relates to fatty acid acifran derivatives; compositions comprising an effective amount of a fatty acid acifran derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid acifran derivative.
US6946121 Composition in particular cosmetic or dermatological composition, containing oligosaccharides and preparation method and cosmetic treatment method The invention concerns a composition comprising at least a first constituent which is an oligosaccharide of formula (I) containing 3 to 5 oside units and having at least a D-galactose unit bound by an α[1-6] bond with a sucrose unit. The invention is characterized in that in said sucrose unit R1, R2, R3, R4, independently of one another represent a hydrogen atom, an alkyl group containing 1 to 10 carbon atoms and optionally having at least an unsaturation, a sulphate function or else an ose and, at least a second constituent which is a molecule positively charged with a physiological pH and stimulating pinocytosis or a molecule stimulating membrane penetration.
US20100061960 Amido Anti-Viral Compounds, Compositions, And Methods Of Use Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.
CN103520124A Levofloxacin hydrochloride tablet and preparation method thereof The invention discloses a levofloxacin hydrochloride tablet and a preparation method of the levofloxacin hydrochloride tablet. The preparation is prepared by blending and tabletting medicine-containing particles, citric acidenteric particles and a lubricant, wherein the citric acidenteric particles is prepared by dissolving the citric acid and the polyvinyl acetatephthalic acid ester in ethyl alcohol. According to the invention, the citric acid is wrapped in an enteric material and is not dissolved in the stomach, the citric acid is dissolved and released in the intestines, so that the alkalinity of the intestinal juice is reduced, the levofloxacin hydrochloride is enabled not to be separated out, and therefore, the bioavailability of the medicine is improved.
CN101766583B Medicinal effervescent tablet for treating cough and preparation method thereof The invention discloses a medicinal effervescent tablet for treating dry cough and persistent cough due to acute upper respiratory tract infection and acute bronchitis and a preparation method thereof, wherein, the effervescent tablet is composed of active levodropropizine, pretreated effervescent disintegrant, filler, flavouring agent, colorant and water-soluble lubricant.
US20080125429 1-{[5-[4-(Methylsulfonyl)phenoxy]-2-(2-pyridinyl)-1H-benzimidazol-6-yl]methyl}-5-thioxo-2-pyrrolidinone;glucokinase activator; antidiabetic agents; obesity; prevention of retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis; antiischemic agents; cardiotonic agents A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.
US20090010909 Novel GPCR and methods of use of the same The present invention relates to methods of identifying antagonists of GPR22, a G protein-coupled receptor (GPCR) and related compositions and methods. Antagonists of GPR22 are useful as therapeutic agents for the treatment of ischemic heart disease, including myocardial infarction, post-myocardial infarction remodeling, and congestive heart failure.
WO2011161031A1 Benzotriazolodiazepine compounds inhibitors of bromodomains Benzodiazepine compounds, pharmaceutical compositions containing such compounds and to their use in therapy.
CN103239412A Pharmaceutical composition comprising loperamide or hydrochloride thereof and preparation method thereof The invention discloses a stable granular pharmaceutical composition comprising loperamide or hydrochloride thereof. The pharmaceutical composition also comprises an adhesive which has the effect of stabilizing the loperamide or hydrochloride. Meanwhile, the invention discloses a method for preparing the stable granular pharmaceutical composition. The granular pharmaceutical composition also can serve as a medicine which is in clinical urgent need of development and has a good effect on children acute dysentery.
CA2309353C Surfactant-based antimicrobial compositions and methods for using same Antimicrobial compositions and methods for preparing and using same are provided. The antimicrobial compositions are surfactant-based and contain certain benzalkonium chloride homologs. The compositions are useful in treating infections in animals and humans, and can be applied to areas including the skin, nails, and mouth.
WO2007141026A1 Use of a polyphenol in the treatment of the metabolic syndrome and endothelial dysfunction or other vascular sequellae. The invention relates to the use of a polyphenol in the manufacture of a nutriceutical, a food, a food supplement or a medicament for the prophylactic or therapeutic treatment of endothelial dysfunction or the Metabolic Syndrome and other vascular sequellae. The invention further relates to a composition comprising at least one polyphenol and to a method for preparing such composition.
US20080125448 Quinazoline Based EGFR Inhibitors Containing a Zinc Binding Moiety The present invention relates to quinazoline containing zinc-binding moiety based derivatives that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer.
CN102552591A Application of pain-relief anti-inflammation ointment to curing cerebral edema of contusion and laceration of brain The invention discloses application of a pain-relief anti-inflammation ointment to curing cerebral edema of contusion and laceration of the brain in pharmacopoeia medicines. The pain-relief anti-inflammation ointment is externally applied to a running area with neck artery bifurcation serving as the center. The pain-relief anti-inflammation ointment has effects of anti-microbial and anti-microbial, can effectively cure nerve dysfunction caused by cerebral contusion and relieve symptoms including headache, nausea, vomit and the like caused by the cerebral edema and increased intracranial pressure, and has obvious effects.
CN101185642B Glucosamine lysine selenium salt and production process The invention discloses an aminoglucose lysine selenium salt and the preparation method thereof. The preparation methods include the steps of aminoglucose preparation, aminoglucose selenite preparation, and reaction of aminoglucose selenite with lysine to obtain aminoglucose lysine selenium salt. The invention has the advantages of simple technique, easy accessed crude materials and low costs. The product in the invention is a novel selenium coordination compound, generated by combining diatomic selenious acid radical negative ion with aminoglucose and lysine respectively; the product can improve effective absorption and antioxidation of organic selenium.
US8501774 Oxazolidinone-quinolone hybrid antibiotics The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
EP1106175B1 Anti-inflammatory ascorbic acid derivatives Anti-inflammatory analgesics which contain as the active ingredient ascorbic acid derivatives represented by general formula (I) or salts thereof, exhibit favorable anti-inflammatory and analgesic effects and are excellent in storage stability, safety to the skin and the percutaneous absorbability of the active ingredient wherein at least one of R1, R2 and R3 represents linear or branched C1-20 alkyl, alkylcarbonylmethyl, alkoxycarbonylmethyl, allylalkyl, acyl, sulfate or phosphate while the remainder represent hydrogen.
CN1605337A Application of cnidium fruit element in the preparing process of medicine for preventing and treating Sexual dysfunction The present invention discloses the application of cnidiadin in preparing medicine for preventing and treating sexual dysfunction.
EP1094799B1 Apomorphine-containing dosage forms for ameliorating male erectile dysfunction Psychogenic impotence can be ameliorated without substantial undesirable side effects by administration of apomorphine and an antiemetic agent in an amount sufficient to substantially reduce nausea symptoms associated with the use of apomorphine.
CN102140066A Medicinal application of benzyl chloride tertiary amine dibromo antimicrobial compounds The invention relates to benzyl chloride tertiary amine dibromo antimicrobial compounds and pharmaceutically-acceptable salts thereof, and also relates to application of the benzyl chloride tertiary amine dibromo antimicrobial compounds and the pharmaceutically-acceptable salts thereof or solvates thereof or mixtures thereof in the preparation of antimicrobial medicaments. The benzyl chloride tertiary amine dibromo compounds have a structure shown by a formula I.
EP1981880A2 Use of 4-imidazole derivatives for cns disorders The present invention relates to the use of compounds of formula (I) wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, phenyl, S-phenyl or O-phenyl, which are optionally substituted by lower alkoxy or halogen, or is benzyloxy, C(O)O-lower alkyl, cycloalkyl, or is lower alkyl or lower alkoxy substituted by halogen; Ar is aryl or heteroaryl, selected from the group consisting of phenyl, naphthyl, pyridinyl, benzofuranyl, dihydrobenzofuranyl or pyrazole; R1/R1' are independently from each other hydrogen, hydroxy, lower alkyl, lower alkoxy or are phenyl or benzyl, which are optionally substituted by halogen; R2 is hydrogen or lower alkyl; n is 1, 2, 3 or 4; and to their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms for the preparation of medicaments for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
CN101342143A Preparation of antineoplastic drug docetaxel injection The invention relates to a preparation process of anticancer drug docetaxel injecta, which is applied to the field of chemical medicine. The product preparation process comprises that 20g to 25g of docetaxel is weighed precisely according to the formula dosage and is added into 2000ml to 3000ml of absolute ethyl alcohol to be stirred till being dissolved completely, and then 500ml to 800ml sterilized polysorbate 80 is added to be stirred for mixing till clarification; the mixture is filtered two times with a microporous filtering film and a degermation and heat-extraction filter under the aseptic condition, and then is subpackaged in vials after is in sure of asepsis and no heat source, and the half cap-pressing is carried out on line; the mixture is dried in vacuum under the prescriptive temperature, vacuum degree and time and then is sealed after the ethanol is removed, and finically the cap is pressed. The process has complete sterilization, simple heat-extraction preparation flow and low cost, is easy to be accepted by the patients, alleviates the pain of the patients, and has obvious healing efficacy and safe and reliable medication.
WO2013078764A1 Applications of 1β-hydroxy isoalantolactone in preparing medicines against rheumatoid arthritis The present invention provides applications of 1β-hydroxy isoalantolactone in preparing medicines against rheumatoid arthritis. The structural formula of the 1β-hydroxy isoalantolactone is as shown by formula (I). The 1β-hydroxy isoalantolactone can obviously suppress the extent of the disease and disease incidence, decrease TNF-α, IL-17 and IFN-γ in spleen cell supernatants, and suppress secretion of TNF-α, IL-17, and IFN-γ. The 1β-hydroxy isoalantolactone can be used for preparing medicines for treating rheumatoid arthritis. The active ingredient in the medicines is the 1β-hydroxy isoalantolactone, and is made with conventional pharmaceutically acceptable carriers into pharmaceutical compositions comprising tablets, dispersible tablets, lozenges, orally disintegrating tablets, sustained release tablets, capsules, soft capsules, dropping pills, granules, injections, powders for injection, and aerosols.
WO2013085276A1 Film for oral administration containing mirodenafil or pharmaceutically acceptable salt thereof The present invention provides a film preparation for oral administration comprising mirodenafil or a pharmaceutically acceptable salt thereof - preferably, the free-base form of mirodenafil. The present invention also provides a method for manufacturing a film preparation for oral administration comprising mirodenafil or a pharmaceutically acceptable salt thereof - preferably, the free-base form of mirodenafil.
CN1634584A Anti-cancer medicine composition containing antimetabolite An anticancer pharmaceutical composition composed of pharmaceutic adjuvant and anti-metabolism medicine is disclosed. Wherein, the anti-metabolism medicine can effectively destroy DNA and/or protein synthesis and repairing function inside the tumor cell so as to inhibit the tumor cell growth, while the pharmaceutic adjuvant can mainly be biological compatible, degradable and absorbable macromolecule polymer, which can make the anti-metabolism drug to release slowly in the local tumor region in the degradation and absorption process, therefore it can both decrease considerably the whole body toxic reaction and sustain the local tumor effective drug level.
US20110144060 Substituted pyrazinone melanin concentrating hormone receptor-1 antagonists and methods The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
EP1515728A2 Use of orally-available prostacyclin derivatives for the production of a medicament for the treatment of disease states associated with bone marrow oedema The invention relates to the use of orally-available prostacyclin derivatives for the production of a medicament for the treatment of disease states associated with bone marrow oedema.
EP2109611A1 7-azaindole derivatives and their use in the inhibition of c-jun n-terminal kinase The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and the use in medicine and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.
US20120330224 Gas conditioning A compound for the manufacturing of a medicament for reducing or preventing mesothelial cell damage includes a mixture of a carrier gas and between 1 volume percent and 29 volume percent of nitrous oxide gas (N2O) and can be used for prevention of adhesion formation, pain reduction, reducing or preventing acute inflammation, reducing or preventing CO2 resorbtion or reducing tumor cell implantation upon surgery.
WO2009155689A1 Nitric oxide device and method for wound healing, treatment of dermatological disorders and microbial infections The present disclosure provides a device having a casing with a barrier surface and a contact surface and a composition in the casing having a nitric oxide precursor and an isolated enzyme or live cell expressing an endogenous enzyme, for converting the nitric oxide gas precursor to nitric oxide gas or having activity on a substrate that produces a catalyst that causes the conversion of the nitric oxide gas precursor to nitric oxide gas. The present disclosure also provides methods and uses for treating wounds, microbial infections and dermatological disorders and for preserving meat products.
US20090253710 NMDA Receptor Antagonists for Neuroprotection Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3−R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(═O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.
WO2013170756A1 Applications of dopac in preparing antitumor drugs The present invention provides applications of 3,4-Dihydroxyphenylacetic acid (DOPAC) or medically acceptable salt, solvolyte, or polycrystal thereof in preparing drugs for preventing and/or curing tumors. Experiments in vivo and vitro indicate that DOPAC can suppress multiple types of tumors such as lung cancer, breast cancer, cervical carcinoma, nephroblastoma, nasopharyngeal carcinoma, laryngeal carcinoma, and neuroblastoma, and has broad-spectrum antitumor functions. This type of compounds are derived from natural drugs, and hopefully provide new choices for clinical treatment.
WO2011017125A1 Trisubstituted boron-containing molecules This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections.
CN103690499A Stable crystalline form I agomelatine tablets and preparation method thereof The invention discloses stable crystalline form I agomelatine tablets and a preparation method thereof. The method comprises the following steps: adding one or several protective agents into purified water, stirring, heating to the temperature of 35-40 DEG C, dissolving until the mixture is clarified, cooling to room temperature, adding crystalline form I agomelatine, and uniformly stirring to obtain a protective agent containing the crystalline form I agomelatine; uniformly mixing partial pharmaceutical excipients, adding the protective agent containing the crystalline form I agomelatine, and performing wet mixed granulating and drying to obtain granules containing the crystalline form I agomelatine; finally, adding the rest pharmaceutical excipients for uniformly mixing according to a ratio, and tabletting. According to the preparation method, the condition that the crystalline form I is not changed in the tablet preparation process can be fully guaranteed; the stability of the crystalline form I and related substances is high, and the requirement of large-scale production can be completely met.
US7115661 Methods and compositions for mitigating pain Methods and therapeutic compounds for treating pain, mitigating inflammation, effecting analgesia and/or effecting sedation in a subject are described. A subject is administered an effective amount of a therapeutic compound which is a nitrate ester. Novel pharmaceutical compositions are also described.
EP2712613A1 Vitamin K1 and uses thereof The present invention relates to vitamin K1 and uses thereof, to pharmaceutical formulatins comprising vitamin K1 and uses of such formulations, and furthermore to methods of treatment involving the administration of vitamin K1 or of pharmaceutical formulation comprising vitamin K1.
WO2007038372A1 Phenylethylamine analogs and their use for treating glaucoma Phenylethylamine analogs useful for treating glaucoma are disclosed.
EP2392323A1 Prostate cancer progression inhibitor and progression inhibition method A prostate cancer progression inhibitor comprises 4-(4-cyano-2-{[2-(4-fluoro-1-naphthyl)propanoyl]amino}phenyl)butyric acid, a salt thereof, a solvate thereof, or a prodrug thereof. 4-(4-Cyano-2-{[2-(4-fluoro-1-naphthyl)propanoyl]amino}phenyl)butyric acid is useful as a prostate cancer progression inhibitor because this butyric acid has, for example, a growth inhibiting effect and a hormone responsiveness recovering effect on prostate cancer that has acquired hormone resistance.
WO2014094527A1 Compounds and methods for the treatment of erb b2/neu positive diseases Disclosed herein are anti-ERB B2/NEU antibodies conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods relating to the preparation and uses of such drug conjugates to treat ERB B2/NEU positive cells in cancers are provided.
EP2051710B1 Compositions and methods for treating, reducing, ameliorating, or alleviating posterior-segment ophthalmic diseases A composition for treating, reducing, ameliorating, or alleviating a back-of-the- eye condition or disorder that has an etiology in inflammation comprises a dissociated glucocorticoid receptor agonist ('DIGRA'). The compositions also can include other anti-inflamatory agents, anti-angiogenic agents, or combinations thereof. The composition can be formulated for topical application, injection, or implantation. The composition can be administered alone or in combination with another procedure chosen to enhance the outcome of the treatment.
CN102114219A External ointment for dispersing swelling, relieving pain and diminishing inflammation The invention discloses an external ointment for dispersing swelling, relieving pain and diminishing inflammation, which comprises the following constituents: 10-25 grams of szechuan lovage rhizome, 20-40 grams of savia miltiorrhiza, 15-25 grams of fructus gardeniae, 10-25 grams of safflower, 10-25 grams of pricklyash peel, 15-25 grams of turmeric, 10-20 grams of camphor, 10-20 grams of asarum, 20-25 grams of fennel, 10-25 grams of Japanese ampelopsis root, 10-25 grams of moutan bark, 10-25 grams of phellodendron, 20-25 grams of tea leaf and 50-150 grams of sesame oil. The medicine constituents in the external ointment can quickly penetrate into skin, and have remarkable effects of effectively inhibiting pain factors, dispersing the swelling and relieving the pain and strong functions of easing the pain, dispersing the swelling and resisting the inflammation and rheumatism no matter chronic pain such as waist and back pain and the like or acute pain such as sprain, pulling injury and the like. The ointment has the advantages of simplicity for use, convenience, safety and no side effect.
EP2158914A2 Use of estriol in low doses The invention relates to the use of low doses of estriol by vaginal route for treatment and/or prevention of urogenital atrophy due to estrogen deficit in women.
US6864282 9,11-cycloendoperoxide pro-drugs of prostaglandin analogues for treatment of ocular hypertension and glaucoma 9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.
CN102344443A Open-loop maleimide compound utilizing click chemosynthesis and application in treating diseases thereof The invention relates to an open-loop maleimide derivative utilizing click chemosynthesis and having kinase inhibitory activity. The structural general formula of the open-loop maleimide derivative is shown in A. In the formula, R1 and R2 can be a hydrogen atom, alkyl, a naphthenic base, heterocyclic alkyl, heterocyclic alkyl, alkenyl, cyclohexenyl, heterocyclic alkenyl, heterocyclic alkenyl, chain alkynyl, heterocyclic alkynyl, heterocyclic alkenyl, aryl, heterocyclic aryl or glycosyl, wherein R3 is the hydrogen atom or methyl. The open-loop maleimide derivative comprises a compound obtained through performing substitution derivatization or bridging derivatization on the R1 and/or the R2 alternately and repeatedly, and also comprises a compound obtained through performing single-bond linked derivatization on the R1 and the R2. The compounds can be applied to preparing drugs for treating neurodegenerative diseases and cancers.
CN101735113A Urea derivatives, preparation method and use thereof The invention provides urea derivatives, which have the following general formula. In the formula, R is H or nitroso, R2 is 5-chloro-2-hydroxyphenmethyl or 3,5-dichloro-2-hydroxyphenmethyl, and R3 is p-methylphenyl, p-fluorophenyl, p-methoxyphenyl, p-chlorophenyl, p-bromophenyl, 2,4-difluorophenyl, 2-chlorophenyl, 2-(N-morpholinyl)ethyl, 3-(N-morpholinyl)propyl, n-dodecylamino, n-hexadecylamino or n-octadecylamino. The urea derivatives have an obvious inhibiting effect on the cancer cell strain (KB) of the epicuticle of human oral cavity and human leukemia cell strain (K562). Thus, the urea derivatives can be applied to the preparation of antineoplastic drugs. The invention discloses a preparation method of the urea derivatives.
US20110300227 Malignant neoplasm treatment protocol Methods, compositions, and strategies for the treatment of malignant neoplasms are presented herein. The treatment modalities are directed towards exploiting characteristics of cancer cells as well as correcting defective biochemical pathways and systems in the body.
WO2014162303A1 Use of a dietary fibre supplement in a food formulation Use of dietary fibre material extracted from sugarcane in the manufacture of a food product that is formulated to ameliorate the effects of intestinal tract disorders such as Coeliac's disease and Irritable Bowel Syndrome (IBS).
WO2005120491A1 Remedy or preventive for inflammatory bowel disease A remedy for an inflammatory bowel disease, in particular, ulcerative colitis and a remedy or a preventive for Crohn’s disease comprising nafamostat mesilate, the safety of which has been already proved, as the active ingredient. The details are as follows. (1) A remedy or a preventive for an inflammatory bowel disease comprising nafamostat mesilate as the active ingredient. (2) A remedy or a preventive as described in the above (1) wherein the inflammatory bowel disease is ulcerative colitis. (3) A remedy or a preventive as described in the above (1) wherein the inflammatory bowel disease is Crohn’s disease. (4) A remedy or a preventive as described in the above (1) which is to be used as a combination with 5-ASA.
US20120149683 Substituted aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
US20100310621 Controlled Iodine Release Particle Micro-Biocide A controlled release molecular iodine biocide for use in human cavities especially the vaginal, penile canal, nasal passages and rectum. Particles can be functionalized with epithelial cell binding molecules and lymphocyte-binding molecules attached to their surfaces. Half of all the particles can contain pH buffer salts that control pH to between around pH 3.5 to pH 4.5. A second half of the particles can contain Iodide and iodate salts. When pH particles and iodate/iodide particles are bound next to each other, molecular iodine is released in a controlled fashion. Molecular iodine is effective biocide. In an alternate embodiment, there can be two distinct populations of particles, one with epithelial cell binding molecules and one with lymphocyte-binding molecules. Again, half of all the particles can contain a pH buffer and half iodide and iodate salts.
CN102018767A Method for preparing celandine liquid extract and preparation containing celandine liquid extract The invention discloses a method for preparing a celandine liquid extract and a preparation containing the celandine liquid extract. The celandine liquid extract is prepared through acid liquid mixing, hot dipping, filtering and concentration, has simple process and low cost and is easy to industrialize. The preparation prepared by proportionally adding dried alum, calcined oyster powder and other auxiliary materials has exact curative effects on gastric ulcer, duodenal ulcer and the like, and can effectively alleviate the symptoms of gastral cavity pain, acid regurgitation and the like caused by the same. The preparation has obvious economic benefit and social benefit and has broad application prospect.
CN103127003A Omeprazole enteric micropelets and capsule as well as preparation method thereof The invention discloses omeprazole enteric micropelets and a capsule prepared from the same. The capsule is prepared by dispersing omeprazole liposome in an enteric coating material aqueous solution, coating blank pellets and then coating an enteric layer so as to obtain the enteric micropelets, and filling the enteric micropelets into the capsule. By utilizing the capsule, the stability of the omeprazole enteric micropelets is obviously improved, and moreover, the usage amount of a plasticizing agent is reduced; and the capsule is simple in technological operation and suitable for industrial production.
CN101098852A Glycogen phosphorylase inhibitor compounds and pharmaceutical compositions thereof The invention relates to glycogen phosphorylase inhibitor compounds, pharmaceutical compositions of these compounds, methods of treatment using the pharmaceutical compositions to treat diabetes, conditions associated with diabetes, and/or tissue ischemia, including myocardial ischemia, and processes for making the compounds.
EP2143716A1 Pyrazine derivatives, methods of use, and methods for preparing same The present invention relates to methods of making pyrazine derivatives.
US20120190633 Monophosphorylated lipid a derivatives The present invention provides for monophosphorylated lipid A derivatives and carbohydrate derivatives that are useful as agents in the treatment of diseases and conditions, including cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I-IV. In addition, methods for the treatment of cancers are provided.
CN101705175A Cordial for preventing diseases and epidemics and production method The invention discloses a cordial for preventing diseases and epidemics and a production method. The cordial comprises the following raw materials: rhizoma atractylodis, Chinese mugwort, Chinese arborvitae twig, pricklyash peel, peach seed, mint, purple perilla, honeysuckle flower, platycodon root, dark plum fruit, unripe liquoric root, vitamin C, crystal sugar and white wine. The production method produces the cordial according to the components and the technique.
US20050059589 Such as cutaneous, ocular, nasal and bronchial allergic disease; interleukins and tumor necrosis factor receptors; competitive binding Methods and compositions for treating allergic reactions, including cutaneous, ocular, nasal and bronchial allergic disease, are disclosed. Interleukin-1 and Tumor Necrosis Factor receptors, and analogues thereof, are employed which bind the respective effector competitively and thereby suppress allergic reactions.
CN102151255A Application of resveratrol in preparing medicines for preventing and treating radiation-induced bone marrow suppression The invention provides application of a polyphenol compound, such as resveratrol, which is wide in sources, safe and effective, and economic and applicable, in preparing medicines for preventing and treating radiation-induced bone marrow suppression. Results show that the resveratrol has remarkable protection effects on radiation-induced bone marrow cell injuries, such as peripheral blood leukocyte reduction, hypoplastic bone marrow, aplastic anemia and function reduction, and the resveratrol can be used in large dose and has no remarkable toxic and side effects.
WO2012164578A1 Compositions and methods for preparing immediate release formulations of nilotinib Pharmaceutical compositions comprise nilotinib or a pharmaceutically acceptable salt thereof and a process for the preparation of the same. Methods of using such compositions treat subjects suffering from Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML). A process for preparing dry-granulated pharmaceutical composition of nilotinib comprising compacting nilotinib hydrochloride alone or mixing with one or more of pharmaceutically acceptable excipient(s) by roller compactor or slugging; sizing the compacts or slugs into granules by milling; mixing the granules with one or more of pharmaceutically acceptable excipients to form the composition.
CN1672683A Hyperlipidemia treating composition The present invention provides one kind of hyperlipidemia treating composition and features that the hyperlipidemia treating composition contains Acipimox and Lovastatin in effective treating amount and in the weight ratio of 5-40, preferably 20. The hyperlipidemia treating composition has high synergistic hyperlipidemia treating effect and no obvious toxic side effect.
CN1569838A Meptazinol ortho-propionyloxy-cis-benzyl acrylate and its salts and their production method The invention relates to meptazinol ortho-propionyloxy-cis-benzyl acrylate and its salts and their production method, wherein meptazinol is reacted with key intermediate compound ortho-propionyloxy-cis-benzyl acrylic acid at the presence of 4-dimethy aminopyridine catalytic dehydration into phenolic ester, then into salts.
US20110237627 Methods of synthesizing anatabine Anatabine is obtained by reacting benzophenoneimine with 3-aminomethyl pyridine to form benzylhydrylidene-pyridin-3-yl-methyl-amine. The benzylhydrylidene-pyridin-3-yl-methyl-amine is treated with a non-nucleophilic base and a dielectrophile, such as cis-1,4-dichloro-2-butene, followed by acidification, then basification, to provide anatabine. The resulting anatabine is substantially free from contaminants and displays good stability. In an alternative embodiment, the benzylhydrylidene-pyridin-3-yl-methyl-amine may be used in the synthesis of other alkaloids such as anabasine, nornicotine, N-methylanabasine, and anabaseine.
US20050176702 1,8-Annelated quinoline derivatives substituted with carbon-linked triazoles as farnesyl transferase inhibitors This invention comprises the novel compounds of formula (I) wherein r, s, A, X, Y1, Y2, R1, R2, R3, and R4 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
US20130018085 iRNA Agents Targeting VEGF The features of the present invention relate to compounds, compositions and methods useful for modulating the expression of vascular endothelial growth factor (VEGF), such as by the mechanism of RNA interference (RNAi). The compounds and compositions include iRNA agents that can be unmodified or chemically-modified.
CN101219134A Use of chlorogenic acid in preparing antipyroxic medicamentor foods The invention provides an application of chlorogenic acid in preparation of antihypoxic or antihypoxic food, which also provides a medical composition used for anti-hypoxia with the chlorogenic acid as an active ingredient. The chlorogenic acid which is discovered to have the antihypoxic effect through experiment can prevent lean-oxygen hypoxia and relieve histotoxic hypoxia caused by the biological dysoxidation with certain effect on hypokinetic hypoxia and circulatory hypoxia. The long-term administration of the chlorogenic acid has the advantage of low-toxicity, thus applying to the preventive and therapeutic medication.
CN103382213A 17-(2', 5'-disubstituted oxazolyl)-androstane-4, 16-diene-3-ketone, and preparation method and applications thereof The invention discloses 17-(2', 5'-disubstituted oxazolyl)-androstane-4, 16-diene-3-ketone, and a preparation method and applications thereof. The preparation method comprises a following step: 17-ethynyl-androstane-4, 16-diene-3-ketone and a nitrile compound are subjected to catalytic reaction in the presence of oxidizing agent 8-methylquinoline-N-oxide and gold catalyst so as to obtain 17-(2', 5'-disubstituted oxazolyl)-androstane-4, 16-diene-3-ketone. The preparation method is simple and is suitable for industrial production; speed is fast; and yield is high. Obtained 17-(2', 5'-disubstituted oxazolyl)-androstane-4, 16-diene-3-ketone is used as an active ingredient in preparation of antitumor drugs which possess inhibitory activity on human hepatoma cells, human lung cancer cells, human cervical carcinoma cells, human breast cancer cells and human prostatic cancer cells.
CN102961368A Curcumin nanosuspension and preparation method thereof The invention belongs to the technical field of medicine, and discloses curcumin nanosuspension and a preparation method of the curcumin nanosuspension. As curcumin is poor in stability, small in solubility and low in oral bioavailability, popularization and use of the curcumin are restricted. The curcumin nanosuspension disclosed by the invention is characterized by containing the curcumin, piperine, and zein, and the mass ratio of the curcumin to the piperine to the zein is 10 to (8-9) to (1-2). The preparation method of the curcumin nanosuspension disclosed by the invention is mild in condition, simple and controllable, and the curcumin achieves high oral bioavailability.
CA2849559A1 Methods of modulating cell surface receptors to prevent or reduce inflammation The invention includes a method of distinguishing among oral bacteria species to determine whether a species is orally deleterious. Such method includes contacting at least one bacterium or portion of bacterium of a species of oral bacteria a gingival cell; and detecting the presence of an indicator compound. The substantial absence of an indicator material signifies that the species of bacteria is not a deleterious species. Also included within the scope of the invention are methods for determining the anti-inflammatory effect of an agent. Such methods include contacting the cell with the agent in the presence of a deleterious bacterium or portion of such bacterium and detecting the presence of an indicator compound. The substantial absence of an indicator material signifies that agent is an anti-inflammatory agent.
CN101601758A Preparation method of kuhseng anti-itch wine The invention discloses a preparation method of kuhseng anti-itch wine. The eczema and itching in scrotum and anus can be eliminated within short time by using the method. The method is realized by adopting the following technical scheme: grinding alum into 200 meshes of fine powder for later use, mixing and crushing kuhseng, Xi xian cao, broom cypress fruit and cortex dictamni radicis into 100 meshes of fragments, putting the fragments together with alum fine powder in a jar stored with white wine, stirring for 10 minutes, and sealing the jar for 7 days, taking out and then filtering to obtain the finished medicinal liquor.
WO2008124393A1 Benzothiazole derivatives and their use as protein kinase inhibitors The invention provides compounds of formula (1 ) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of AIk, AbI, Aurora-A, B-Raf, Bcr-Abl, BRK, BIk, Bmx, c-Kit, c-RAF, cSRC. CSK, FLTl, Fms, Fyn, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα. p38 (p38 MAP kinase, SAPK2α), Src, SIK, Syk, Tie2 and TrkB kinases. FORMULE (I)
US7022729 For treating central nervous system disorders, immunomodulatory disorders, antimalaria, viral disease of Borna virus, Hepatitis; a 6-azatricyclo(6.3.1.01,6)dodecane derivatives Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.
WO2013024067A1 Use of antioxidants for improving animal health The invention relates to a new use of antioxidants for improving animal health. In particular, as a result of using antioxidants and also substances with an antioxidative effect, an increase or improvement in the endogenous radical defence system, a reduction in inflammatory processes and/or a prevention of and/or reduction in fertility problems is achieved.
CN102512427A New use for ER (estrogen receptor) antagonist The invention discloses a new use for an ER (estrogen receptor) antagonist, wherein the new use is an application in preparation for a medicine used for treating the paclitaxel resistance of tumour cells, the tumour is breast cancer, and the ER antagonist is ER antagonist ICI182,780. Experiment confirms that the high-level expression of ER (estrogen receptor) is an important related index of the medicine resistance of breast cancer cells; the ER antagonist has the advantages of inhibiting the expression level of ER protein and blocking the influence of estrogen on the occurrence and development of breast cancer; and the new use for the ER antagonist exerts good function of reversing the medicine resistance of tumour in paclitaxel-resistant breast cancer cell model, and has wide application prospect in medicine used for treating the paclitaxel resistance of human breast cancer.
CN101537155A Mongolian preparation for tonifying kidney, invigorating spleen and relieving mental stress and preparation method thereof The invention discloses a Mongolian preparation for tonifying the kidney, invigorating the spleen and relieving mental stress and a preparation method thereof. The Mongolian preparation is formed by preparing polygonatum, topaz, lucid asparagus, trichosanthes root, water chestnut, white brain sand, natural salt, halitum violaceum, sophora flavescens ait, nutmeg, clove, galangal, long pepper, round cardamon seed, cane sugar, fresh milk, honey, butter and other raw materials, and has the effect of preventing Heyi, nourishing and building the body, and invigorating yang (tonifying the kidney, invigorating the spleen and relieving the mental stress), and can be used for treating various symptoms like weakness with age, limb weakness, waist soreness and leg pain, kidney coldness and kidney deficiency, dizziness and tinnitus, dreaminess and ahypnosis, uneasiness, Heyi centralization and the like. The invention has the advantages of remarkable treatment effect, convenient taking and no toxic side effect.
WO2014045283A1 Restoration of the cftr function by splicing modulation The present provides oligonucleotides capable of binding to and modulating the splicing of the pre-mRNA of the CFTR gene, compositions comprising said oligonucleotides, kits comprising said compositions, and uses thereof. In particular, the present invention provides compositions of oligonucleotides useful in methods for suppressing exon 10 skipping optionally in combination with additional CFTR therapeutics.
EP2403839A2 Neurotrophin mimetics and uses thereof The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
WO2013010573A1 Compounds with matrix-metalloproteinase inhibitory activity The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention.
US8372395 Nano-emulsion composition of coenzyme Q10 The present invention provides a nano-emulsion composition of CoQ10 comprising 5 to 20 wt. % of CoQ10, 1 to 5 wt. % of ethanol, 1 to 5 wt. % of lecithin, 20 to 30 wt. % of caprylic/capric glyceride or vegetable oil(s), 10 to 20 wt. % of glycerin, 1 to 15 wt. % of coemulsifier(s) and the balance of water. The present invention also provides a nano-emulsion composition of CoQ10 comprising 5 to 20 wt. % of CoQ10, 1 to 5 wt. % of ethanol, 20 to 30 wt. % of caprylic/capric glyceride or vegetable oil(s), 1 to 25 wt. % of emulsifier(s), 10 to 20 wt. % of glycerin, and the balance of water. The nano-emulsion composition according to the present invention can preferably improve stability, in vivo penetration, absorptiveness and bioavailability of CoQ10.
US20080312305 Imidazoles as Gaba- B Receptor Modulators The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be alkyl or arylalkyl, R2 may be alkyl, R3 may be alkoxy and R4 may be a substituent containing an aryl group.
US20110195937 Oxidized thiophospholipid compounds and uses thereof Novel oxidized thiophospholipids are provided herein, as well as methods for producing same, and uses thereof in treating or preventing an inflammation associated with endogenous oxidized lipids and related conditions. Exemplary oxidized thiophospholipid according to embodiments described herein have the formula: wherein X1, X2, A1, A2, B′, B″, D′ and D″ are as described herein.
US20080039408 Use of Oxypurinol as an Inhibitor of Anti-Neoplastic Agent-Induced Cardiotoxicity The disclosure relates to methods of ameliorating or preventing cardiotoxicity caused by anti-neoplastic agents, such as doxorubicin, by administering to a patient oxypurinol, salt or derivatives thereof, before, during or after administration of the anti-neoplastic agent.
CA2592461A1 Drugs for diseases accompanying changes in total bile acid pool or lipid metabolism disorders and method of screening these drugs A Gpbar1-deficient mouse is constructed and it is examined whether or not Gpbar1 participates in the regulation of bile acid homeostasis and lipid metabolism. As a result, the total bile acid pool is decreased in the Gpbar1-deficient mouse without showing any change in the fecal bile acid level. A female Gpbar1-deficient mouse having been fed with a high fat feed shows a significant increase in body weight compared with a wild type mouse, which is caused by an increase in fat. These facts suggest that Gpbar1 contributes to the regulation of bile acid homeostasis and lipid metabolism.
CN103417567A Smoking cessation medicine and preparation method thereof The invention relates to the field of medicine, in particular to smoking cessation medicine and a preparation method thereof. The smoking cessation medicine comprises activated water and smoking cessation cut tobacco. The activated water is filter liquor obtained by carrying out filter after Nuwa ore is steeped in water for 22-26 hours. The smoke cessation cut tobacco is composed of the following components, by weight, 22-26 parts of cut tobacco, 0.15-0.35 part of saccharin, and 7050-9055 parts of the activated water. The preparation method of the smoking cessation medicine comprises the steps of steeping the Nuwa ore in water for 22-26 hours, and carrying out filter to obtain the activated water; fetching, by weight, 50-55 parts of the activated water, adding the saccharin into the activated water, and carrying out dissolution to obtain a first solution; adding the cut tobacco to the first solution, and carrying out still standing for 4-6 minutes to obtain a mixture; heating 7000-9000 parts of the activated water in weight count to boiling; heating the mixture by using the boiled activated water until the weight percentage of water in the mixture is less than or equal to 5%, and obtaining the smoking cessation cut tobacco. The smoking cessation medicine enables a smoke cessation treatment course to be shortened largely.
US20080161253 Composition for the treatment of nasopharyngeal carcinoma and method of use thereof Disclosed is a novel drug combination which is useful for the treatment of nasopharyngeal carcinoma, said novel drug combination comprising one or more of a farnesyl transferase inhibitor and one or more of an anthracycline.
CN1919205A Pharmaceutical composition comprising oxymatrine and baicalin The invention discloses a drug composition with oxymatrine and baicalin, which is characterized by the following: inhibiting HepG2.2.15 cell from secreting surface antigen and e-antigen of hepatitis B effectively, controlling the quantity of oxymatrine and baicalin between 7:1 and 11:1 with 9: 1 at best.
CN102600087A Injection ambroxol hydrochloride composition The invention relates to an injection ambroxol hydrochloride composition and a preparation method thereof. The injection ambroxol hydrochloride composition comprises ambroxol hydrochloride, sulfobutylether-beta-cyclodextrin and dextran, and has simple ingredients. The injection ambroxol hydrochloride composition obtained by adopting a freezing drying process has a good stability and re-dissolving effect. The preparation method has the advantages of mild conditions, shortened freezing drying time interval and cost saving, and is suitable for mass industrialized production.
CN101791315A Compound monoammonium glycyrrhizinate S pharmaceutical composition and method for preparing high-capacity injection The invention belongs to the technical field of pharmaceutical preparations, in particular to a compound monoammonium glycyrrhizinate S pharmaceutical composition and a method for preparing a high-capacity injection. The composition is a compound monoammonium glycyrrhizinate S sodium chloride injection. The injection is characterized by comprising the following components: 40-160g of monoammonium glycyrrhizinate S, 30-120g of cysteine hydrochloride, 400-1,600g of glycine, 40-160g of anhydrous sodium sulphite, 4-16g of sodium citrate, 900-1,800g of sodium chloride, a proper amount of sodium hydroxide and 100-200L of water for injection. The high-capacity injection is more stable and safer.
CA2095797C Arylacetamides Novel arylacetamides of the formula I see formula I in which Q, R1, R2 and R3 have the meaning stated in Patent Claim 1, have analgesic and neuroprotective properties and bind with high affinity to kappa receptors.
US20080124402 N-(Pyridin-3-Yl)-2-Phenylbutanamides As Androgen Receptor Modulators Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
WO2012051407A3 Molecular containers and methods of making and using same Acyclic CB[n]-type compounds, methods of making such compounds, and uses of the compounds. For example, these compounds can be used as nanocontainers to solubilize pharmaceutical agents. Also provided are compositions and methods of using them for therapy or prophylaxis of a wide variety of conditions for which therapy or prophylaxis is desirable.
EP1015884B1 Methods of identifying molecules that home to angiogenic vasculature in tumors A method of identifying a tumor homing molecule that homes to angiogenic vasculature by contacting a substantially purified NGR receptor with one or more molecules and determining specific binding of a molecule to the NGR receptor, where the presence of specific binding identifies the molecule as a tumor homing molecule that homes to angiogenic vasculature. The invention also provides a method of directing a moiety to angiogenic vasculature in a subject by administering to the subject a conjugate including a moiety linked to a tumor homing molecule that exhibits specific binding to an NGR receptor, whereby the moiety is directed to angiogenic vasculature. In addition, the invention provides a method of imaging the angiogenic vasculature of a tumor in a subject by administering to the subject a conjugate having a detectable moiety linked to a tumor homing molecule that exhibits specific binding to an NGR receptor and detecting the conjugate.
WO2010004816A1 Inhibitor of degranulation of mast cell Disclosed are: an inhibitor of the degranulation of a mast cell, which comprises, as an active ingredient, a substance capable of inhibiting the process of biosynthesis of microRNA from a microRNA precursor, such as a substance capable of inhibiting the expression of Dicer1 gene; a method for inhibiting the degranulation of a mast cell; and a therapeutic agent for a disease induced by the abnormality in a mast cell.
EP2409152A1 Methods for modulating circadian rythms This disclosure described the role of AMPK in circadian rhythms and methods of screening for agents that modulate such rhythms, compositions that are useful for modulating such rhythms and uses thereof.
US20110021475 Compositions And Methods for Treatment Of Fibrosis Methods for the treatment of fibrosis, including liver fibrosis, via administration of FXR agonists are provided.
WO2010075060A2 Methods and compositions for modulating proline levels Methods and compositions for modulating amino acid levels in a subject are provided herein.
CN102846678A Application of ginkgolic acid in weight losing The invention relates to application of ginkgolic acid in weight losing. The ginkgolic acid comprises ginkgolic acid, ginkgol and bilobol and can be obtained from extracts of such parts of the gingko as leaves, fruits, testae and rootstalks by a chemical separation method. A weight reducing medicament or cosmetic contains 0.001-80% of ginkgolic acid by weight percent and pharmaceutically common external preparation substrates or acceptable carriers. The preparation is any one pharmaceutically called external dosage form. Pharmacological experiment studies show that the preparation has the functions of reducing weight, body fat and adipocyte quantity and volume and has the effect of reducing blood sugar and blood fat. Trial results of fat people show that the preparation has the functions of reducing weight and removing fat, is obvious in weight reducing effect, is safe to use and has no effects.
US20110177021 Composition for forming a temporary obstruction and method of forming the same The present invention relates to a method for forming a temporary obstruction of the intestine of a mammal, using a solidifiable composition, said composition being flow-able and solidifiable to form a solid plug at a desired site within the intestine, the structure of said plug being changeable in order to allow for the subsequent, at least partial removal of the obstruction.
WO2013109876A1 Enhanced glycemic control using ad36e4orf1 and akt1 inhibitor This invention generally relates to methods for improving glycemic control by administering an Ad36 composition and an AKT1 inhibitor.
WO2006004507A3 New benzothiazole derivatives useful for treating cns disorders The present invention provides new compounds of formula (I) as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
CN101675923B New usage of zedoary cyclic diolefine The invention relates to a new usage of zedoary cyclic diolefine, in particular to application of zedoary cyclic diolefine in preparing antipyretic, anti-inflammatory or antivirotic medicament, and application thereof in preparing medicament for curing influenza viral pneumonia.
US20120225903 Novel 2-Substituted Quinoline Derivatives, And Method For Preparing Same The invention relates to 2-substituted quinoline derivatives, to a method for preparing same, and to the use thereof for drug production, particularly for treating infections caused by protozoa, such as leishmaniases, trypanosomiases, toxoplasmoses, and/or infections caused by retroviruses such as, for example, HIV or HTLV.
EP2014281A1 Use of inhibitors of sirtuins and/or ampk for the preparation of a medicament for the treatment of polyalanine diseases. This invention relates to the use of inhibitors of sirtuins and/or AMPK for the preparation of a medicament for the treatment of polyalanine diseases, in particular oculopharyngeal muscular dystrophy (OPMD). The invention also relates to methods of identifying compounds which can be useful for treating said diseases.
CN103751175A Application of Chukrasone B in vasodilation drugs The present invention provides an application of Chukrasone B in preparation of vasodilation drugs, and particularly relates to an application of the Chukrasone B in preparation of blood pressure lowering drugs, anti-angina pectoris drugs and other anti-vascular disease drugs. According to the present invention, the uses of the Chukrasone B in vasodilation drug preparation are firstly disclosed; and the skeleton type of the Chukrasone B belongs to a completely new skeleton type, the vasodilation activity of the Chukrasone B is strong, possibility that other compounds provide revelations for the Chukrasone B can not exist, prominent substantive characteristics are provided, and significant progress for Chukrasone B is provided.
CN102784146A Medicinal use of N-phenylquinazolinyl-4-amine derivatives The invention belongs to the field of biological pharmacy, relates to a medicinal use of N-phenylquinazolinyl-4-amine derivatives in preparation of drugs for treating nervous system diseases and especially relates to a medicinal use of N-phenylquinazolinyl-4-amine derivatives in preparation of 5-HT receptor inhibitors. A result of a biological activity test shows that the N-phenylquinazolinyl-4-amine derivatives have effects of inhibiting 5-HT1A receptors closely related to pathological mechanisms of nervous system diseases. The N-phenylquinazolinyl-4-amine derivatives can be used as drug lead compounds, be synthesized into 5-HT receptor inhibitors, and be further used for preparation of drugs for treating schizophrenia, depression and Parkinsonism caused by 5-HT system dysfunction.
US8362005 Monocyclic amide CGRP receptor antagonists Compounds of formula (I): wherein variables B, m, n, J, R4, Ea, Eb, Ec, Re, Rf, RPG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
US20090156631 Controlled Release Compositions Containing Zolpidem The present invention relates to controlled release compositions of Zolpidem or pharmaceutically acceptable salts thereof adapted to release Zolpidem over a predetermined time period, according to a monophasic and/or a biphasic profile of dissolution. The present invention also relates to monolithic matrix based formulations of Zolpidem or pharmaceutically acceptable salts thereof.
WO2007124086A1 Induction of weight loss and the selective inhibition of ptp1b The present invention is directed to the use of compound 1436 for the induction of weight loss in an obese mammal.
WO2012014936A1 Cancer stem cell differentiation inducer Provided is an inducer of the differentiation of a cancer stem cell having resistance to existing therapy methods, which can be effective for the treatment of cancer through the induction of the differentiation of the cancer stem cell. Specifically provided are an inducer of the differentiation of a cancer stem cell which comprises an acetaminophen derivative as an active ingredient and an anti-cancer activity enhancer which comprises an acetaminophen derivative as an active ingredient and can enhance the anti-cancer activity of an anti-cancer agent when used in combination with the anti-cancer agent, wherein the acetaminophen derivative is acetaminophen (p-hydroxyacetamide) or o-hydroxyacetamide.
EP1280801B1 Hydantoin-containing glucokinase activators Hydantoin compounds of the formula: wherein R1 is a five-or-six-membered aromatic heterocyclic ring having one to three heteroatoms selected from nitrogen, oxygen, and sulfur, which ring is unsubstituted or substituted with halo, amino, hydroxylamino, nitro, cyano, sulfonamido, lower alkyl, perfluoro lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, perfluoro-lower alkyl sulfonyl, lower alkyl sulfinyl, or-(R¿5?)n-C(O)-OR6; R2 is a cycloalkyl ring containing from 5 to 7 carbon atoms; which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
WO2007091328A1 Method for treatment of lung cancer [PROBLEMS] To provide a method for the treatment of lung cancer using a therapeutic agent for lung cancer comprising an erbB receptor inhibitor as an active ingredient. [MEANS FOR SOLVING PROBLEMS] A method for the examination of the responsivity to an erbB receptor inhibitor in a patient with lung cancer using amphiregulin (AREG) in the blood as a measure; and a method for the treatment of lung cancer comprising the steps of determining the responsivity to an erbB receptor inhibitor based on the blood AREG level and administering the therapeutic agent selectively to a patient who is expected to have the responsivity. A higher therapeutic effect can be expected by administering an erbB receptor inhibitor to a patient who is predicted to have the responsivity. These methods contribute to the improvement in therapeutic effect of Gefitinib (a commercial name 'Iressa'(trade mark)) or the like on lung cancer.
US20050070572 Sulfone derivatives and their use in the treatment of autoimmune diseases and allergies A compound of formula (I) useful in the treatment and prophylaxis of conditions mediated by s-CD23.
CN101507730B Combination of epigallocatechin-3-gallate and cerubidin and use thereof The invention belongs to the field of medicine and gene engineering, and provides a composition for inhibiting the proliferation of tumor cells. The composition contains epigallocatechin gallate (EGCG) and daunorubicin (DNR), and the mass ratio of the epigallocatechin gallate to the daunorubicin is 600: 1-1: 2. The combination of the EGCG and the DNR, on one hand, ensures that the effect of inhibiting the proliferation of the tumor cells is more obvious than the superposition of single use effects, on the other hand, the combination of the EGCG and the DNR obviously reduces the using amount of the DNR, greatly reduces the cardiac toxicity of the DNR, and strengthens the anti-tumor effect of the DNR at the same time. The EGCG is a natural tea extract, has rich resource and low price, and almost has no toxic side effect after more than one thousand years of drinking, so the combination of the EGCG and the DNR relatively reduces the using amount of the DNR and drug cost. The invention provides a high-efficiency cheap anti-tumor pharmaceutical composition, which improves the inhibition rate of tumor and reduces the treatment cost of tumor patients at the same time.
WO2014157382A1 Sphingosine kinase inhibitor The present invention relates to a sphingosine kinase inhibitor comprising a compound represented by formula (I) [wherein each symbol is as defined in the description] or a salt thereof, and provides a compound useful for the prevention and/or treatment of inflammatory bowel disease and the like.
US20120329853 Microrna-based method for anti-colorectal cancer effects and prognosis of colorectal cancer The present invention discloses a method of providing anti-oncogenic effects in a subject suffered from colorectal cancer. The present invention also discloses a method for screening an anti-colorectal cancer agent. The present invention further discloses a method of determining the prognosis of a subject with colorectal cancer.
US8022219 2-hydroxymethy1-3,4,5-trihydroxy-1-(4-pentyloxybenzyl) piperidine as glucosylceramide synthase (Gcs) inhibitor The present invention relates to the compound 3,4,5-piperidinetriol, 2-(hydroxymethyl)-1-[(4-(pentyloxy)phenyl)methyl]-, (2S,3S,4R,5S), or a pharmaceutically acceptable salt or prodrug thereof, which is useful as an inhibitor of glucosylceramide synthase. The compounds of the Invention are useful for treating various glycolipid storage diseases, such as Gaucher's disease, Sandhoff's disease, Tay-Sacs disease, Fabry disease, and GM1 gangliosidosis; glycolipid accumulation disorders, such as Niemann-Pick disease, mucopolysaccharidoses, mucolipidosis type IV and α-mannosidosis; various cancers that involve abnormal glycolipid synthesis; and various infectious diseases that involve cell surface glycolipids as receptors for the infectious organisms or for their toxins; as well as a variety of other disorders involving glycolipid synthesis, including neuronal disorders, inflammatory diseases, obesity, and the like.
WO2004069139A3 4-aminopyrimidin-5-yl-methanone derivatives for inhibition of cdk4 activity Novel 4-aminopyrimidine-5-one derivatives of the formula (I) wherein R1 and R2 are as defined in the specification, are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds, their use for treating or controlling cancer, to a process of their preparation and to intermediates useful in their preparation.
WO2014059251A1 Enhancement of the immune response The technology described herein relates to compositions and methods for enhancing the immune response and/or reducing T cell tolerance in a subject. In some embodiments, the technology described herein relates to administering inhibitors of two or more of CEACAM1, PD1, and/or LAP to, e.g., synergistically reduce T cell tolerance.
WO2008121065A1 Novel pyrrolidine derivatives as antagonists of the chemokine receptor The present invention relates to new compounds of formula (I) or salts, solvates or solvated salts thereof, wherein Q, X1, R1, R2, R3, R4 and m, n and p are defined as in claim 1, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions comprising said compounds and to the use of said compounds as chemokine receptor antagonist in the treatment of respiratory-diseases, airway diseases, inflammatory diseases, chronic obstructive pulmonary disease (COPD) and asthma.
CN1765362A Composition containing amlodipine and angiotensin II receptor inhibitor The invention relates to the compound medicament of amlodipine or its medicinal acid addition salts and angiotensin II receptor depressor such as Irbesartan and its medicinal salts, reagent kit containing the compound and the method for treating hypertension and individuals including humans with heart danger symptoms by using the compound. The medicinal compound has adding and synergy actions, and can be used for the treatment of stenocardia, atherosclerosis, hypertension and hyperlipoidemia.
US20120135959 Metalloprotein inhibitors containing nitrogen based ligands Provided herein metalloproteinase inhibitors containing nitrogen or mixed nitrogen/oxygen donating zinc binding groups. Also provided are pharmaceutical compositions containing the compounds and methods of treating preventing or ameliorating the diseases associated with metalloproteinase activity using the compounds and compositions.
CN102670810A Drug for treating burn and preparing method thereof The invention relates to a drug for treating burn, which mainly takes phellodendron, akebiaquinata, radix saposhnikoviae, Chinese rhubarb, pseudo-ginseng, gypsum and liquorice as raw materials, wherein the raw materials are repeatedly boiled into liquid medicine with slow fire, the liquid medicine is concentrated into thick paste, and then conventional auxiliary materials are added into the thick paste to prepare tablets, capsules, pills, particles, powder, injections or plasters, which are acceptable pharmaceutically. The drug can cure various types of burns.
CN103191114A Moxifloxacin-containing oral drug solid preparation and preparation method thereof The invention relates to a stable oral drug solid preparation containing moxifloxacin, moxifloxacin hydrochloride and hydrate and mannitol thereof and a preparation method thereof. The preparation method is characterized by comprising the steps of evenly mixing the moxifloxacin, moxifloxacin hydrochloride and hydrate and mannitol thereof and other medicinal carriers, tableting by adopting wet granulation or coating after being tablet-compressed. The method is simple to operate, industrialized mass production can be realized, tablets obtained are tidy and smooth in appearance, the dissolving speed is proper, and the quality is stable.
CN103505415A Medium-chain and long-chain fat emulsion injection and preparation method thereof The invention discloses medium-chain and long-chain fat emulsion injection and a preparation method thereof. The injection is prepared by the following components: every 1000 ml of injection contains 50-200 g of refined linseed oil, 50-200 g of medium-chain oil for injection, 6-18 g of an emulsifier, 15-35 g of an isoosmotic adjusting agent, 0.1-2 g of an antioxidant, and water for injection in balancing amount, wherein the pH value of the injection is adjusted to be 5.0-9.0 by adopting a pH value conditioning agent, and the medium-chain oil for injection is medium-chain triglyceride. The preparation method comprises oil phase preparation, water phase preparation, elementary fat emulsion preparation, homogenization and fine filtration. The medium-chain and long-chain fat emulsion injection provided by the invention is a fat emulsion for injection containing the linseed oil, and has good stability; due to the low content of linoleic acid and the high content of linolenic acid in the medium-chain and long-chain fat emulsion injection, the adverse clinical reactions caused by high content of the linoleic acid in the existing fat emulsion injection are solved; and the medium-chain and long-chain fat emulsion injection has the important efficacy of maintaining lipoprotein balance, reducing blood fat, regulating cholesterol metabolism, dropping blood pressure, resisting thrombus and preventing canceration.
WO2010095767A1 Pyrimidin-4(3h)-one derivatives The present invention relates to a compound represented by a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 represents lower alkyl or the like; R2 represents phenyl or the like; R represents a halogen atom or the like; X represents an oxygen atom or the like; Y1, Y2, Y3 and Y4 represent CH or the like; l represents an integer of from 0 to 3; m and n each represent an integer of 1 or 2; p represents an integer of from 0 to 2; and q represents an integer of from 1 to 3.
WO2010135429A3 Compositions for modulating a kinase cascade and mehtods of use thereof The invention relates to compositions comprising 2-(5-(4-(2- morpholinoethoxy)phenyl)pyridin-2-yl)-Λ/-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5- (4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-Λ/-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-iV- benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
CN103705479A Meloxicam sustained release tablet used for pet and preparation method thereof The invention discloses a meloxicam sustained release tablet used for a pet and a preparation technology thereof. The meloxicam sustained release tablet is stable to release and safe to administrate and comprises solid meloxicam dispersoid, a sustained release material, a filling material, an adhesive, a lubricant and a corrigent. The meloxicam sustained release tablet has the characteristics of convenient administration, rapid and lasting effects and stable curative effects.
CN102085293A Liriope muscari extract with anti-tumor action and preparation method thereof The invention provides a liriope muscari extract with anti-tumor action, which is prepared by a method with the following steps: taking liriope muscari roots as raw materials, extracting the raw materials with ethanol, and extracting the extracting solution with n-butyl alcohol to obtain a crude extract; adding the crude extract into water for dissolving; enabling the crude extract solution to pass through a non-polar macroporous resin column; firstly, eluting with water until the eluent is colorless, and then, eluting with the water solution of the ethanol; and collecting the eluent until the eluent is colorless, thereby obtaining the liriope muscari extract. The invention also provides a preparation method of the liriope muscari extract.
CN103371987A Application of urushiol compound to preparation of drug for inhibiting fibering of kidney tissue The invention provides application of a urushiol compound to preparation of a drug for inhibiting fibering of kidney tissue, and particularly provides a urushiol compound shown in the structural formula 1 and application of medical salt of the urushiol compound to preparation of a drug for inhibiting the fibering of liver tissue. The urushiol compound provided by the invention has a good effect of inhibiting the fibering of kidney tissue and is free of fatal toxic and side effects. The urushiol compound and the medical salt provided by the invention can be prepared into an oral agent or an injection type medical preparation for inhibiting the fibering of kidney tissue.
WO2010118405A2 Compositions and methods for reducing hangover symptoms Compositions and methods for reducing hangover symptoms. Generally, a hangover reducing composition includes one or more plant extracts, such as prickly pear cactus extract, white willow bark extract, milk thistle extract, green tea extract, and combinations thereof. In some cases, the composition further includes supplemental nutrients, such as vitamins and minerals (including electrolytes). Some examples of suitable nutrients include sodium, potassium, magnesium, and vitamins C, B1, B2, B3, B6, and B12. The composition is administered to a person in any suitable form, including as a carbonated soft drink, an energy drink, a tea, a sports drink, a non-carbonated drink, a pill, an elixir, and so forth. In some preferred instances, the composition is formulated as a carbonated soft drink. In order to reduce hangover symptoms, the composition is ingested before, during, and/or after the consumption of a drug, such as alcohol.
WO2014085920A1 Methods for preventing and treating inflammatory skin conditions Methods of treating inflammatory skin conditions comprising topically administering a therapeutically effective amount of aurin tricarboxylic acid (ATA), aurin quadracarboxylic acid (AQA), aurin hexacarboxylic acid (AHA), or a combination thereof are provided. The inflammatory skin conditions may include acne vulgaris, allergic dermatitis, alopecia areata, androgenetic alopecia, atopic dermatitis, dandruff, dermatitis herpetiformis, discoid lupus erythematosus, pemphigus, primary cicatricial alopecia, psoriasis, seborrheic dermatitis, and ultraviolet and thermal burns.
EP1525194A1 Aminoalkyl-substituted aryl compounds and their use as sodium channel blockers This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aminoalkyl-substituted aryl compounds of Formula (I), or a pharmaceutically-acceptable salt or solvate thereof, wherein n, X, Rl, R2 and R3 are defined in the specification. The invention is also directed to the use of compounds of Formula (I) for the treatment of neuronal damage following global or focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of acute or chronic pain, neuropathic pain or surgical pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
EP1806367A2 Polymers containing polysaccharides such as alginates or modified alginates Materials which contain polysaccharide chains, particularly alginate or modified alginate chains. The polysaccharide chains may be included as side chains or auxiliary chains from a backbone polymer chain, which may also be a polysaccharide. Further, the polysaccharide chains may be crosslinked between side chains, auxiliary chains and/or backbone chains. These materials and non-modified or otherwise modified alginate materials are advantageously modified by covalent bonding thereto of a biologically active molecule for cell adhesion or other cellular interaction. Processes for preparation of these alginate materials and methods for using them, particularly for cell transplantation and tissue engineering applications.
US20080152695 Oral/buccal transmucosal delivery methods for electrolyte compositions including xylitol The present disclosure is an oral/buccal transmucosal delivery method which includes, generally, an edible thin film strip including a predetermined volume of xylitol. The edible thin film strip of the present disclosure is preferably comprised of potassium chloride; trisodium citrate; sodium chloride; glucose, and; xylitol.
EP2640392A2 Substituted 4-(selenophen-2(or 3)-ylamino)pyrimidine compounds and methods of use thereof Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.
CN101843599A Oral cephalosporin ester capsule The invention relates to an oral cephalosporin ester capsule which comprises the components: 30-90wt% of cephalosporin ester, 5-50wt% of weak acid salt based on the total weight of the content of the capsule. The cephalosporin ester capsule further comprises filler, organic acid, disintegrating agent and surface active agent.The cephalosporin ester capsule does not exceed the solubility limit of corresponding cephalosporin ester tablets, thus overcoming the defects of low dissolving out limitation of the original cephalosporin ester capsule and not thorough odor masking of other preparations, and having simple technique and low cost.
US20080070900 Administering galantamine or galantamine hydrobromide antidotes to a human at a risk of exposure to parathion or malathion toxicity, subsequently administering atropine as an antimuscarinic agen. A method of treating organophosphorous (OP) poisoning comprising administering to a mammal at risk for OP poisoning an OP poisoning-inhibiting amount of galantamine.
CN102225051A pH sensitive doxorubicin nanoliposome modified by folic acid-carboxymethyl chitosan The invention relates to pH sensitive doxorubicin nanoliposome modified by folic acid-carboxymethyl chitosan and its preparation method. The liposome provided in the invention comprises doxorubicin, phosphatide, cholesterol, vitamin E, folic acid-carboxymethyl chitosan. The prepared liposome has pH sensitivity, tumor targeting performance and long cyclic active targeting drug delivery functions.
US20060148907 Topical antinflammatory preparations of y-terpinene An anti-inflammatory agent comprising from 0.01-1.0% γ-terpinene in a pharmaceutically acceptable vehicle.
EP1291343B1 Hydroxyformamidine derivatives and medicines containing the same Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided. The present invention relates to hydroxyamidine compounds represented by the formula: wherein R<1> represents a group represented by the formula: R<2>-(CH2)m- (wherein R<2> represents a C3-8 cycloalkyl group, a C2-6 alkoxycarbonyl group, a C2-10 alkenyl group, a C2-6 alkynyl group, a substituted or non-substituted aryl group, or the like, and m is an integer of 1 to 8), a group represented by the formula: R<3>-A- (wherein R<3> represents a hydrogen atom, a C1-6 alkoxy group, a C3-8 cycloalkoxy group, or the like, and A represents a straight-chain C2-10 alkylene group which may be substituted with a C1-6 alkyl group or a trifluoromethyl group), or a C3-8 cycloalkyl group, and X represents an oxygen atom or a sulfur atom, or pharmaceutically acceptable salts thereof, and relates to medicines including the same as active ingredients.
CA2843611A1 Compositions and methods for reducing the incidence of equine digestive disorders The present invention encompasses compositions and methods of reducing the incidence of equine digestive disorders.
CN101584754A Medicinal preparation used for liver and gallbladder diseases and preparation method thereof The invention discloses a medicinal preparation used for clearing heat, transforming dampness and soothing liver and gallbladder and used for acute/chronic cholecystitis, biliary tract infection, biliary calculus and the like and a preparation method thereof. The preparation method is characterized in that synthetic bovine bezoar, silymarin, berberine hydrochloride, corydalis root, rhubarb, dandelion, loosestrife and mint oil are used as raw materials, and the raw materials and pharmaceutically acceptable matrix or additive are prepared into dripping pills or soft capsules. The medicinal preparation improves the leaching performance of the medicament, increases the medicament stability, reduces adverse reaction of the medicament, is convenient to carry and take, and is suitable for industrialized production.
US20100062999 Composition extracted from shark cartilage marrow The present invention relates to a composition extracted from shark cartilage marrow. This composition possesses effects of anti-melanoma effect, neutralization of gastric acid, and improvement of blood circulation and comprises Chondroitin Sulfate that is the active component thereof and is 50-60 wt % of the total weight of the composition. Besides, the composition has a molecular weight between 21-100 kilo Daltons and has energy state about 300-350 kilocalories per 100 grams.
US20100305131 Substituted Aminopropionic Derivatives as Neprilysin inhibitors The present invention provides a compound of formula I′; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
WO2008045920A3 Intra-mammary teat sealant formulation and method of using same to reduce or eliminate visual defects in aged cheeses Described is an intra-mammary teat sealant and a corresponding method of forming a physical barrier in the teat canal of a non-human animal for prophylactic treatment of mammary disorders during the animal's dry period. The method includes the step of infusing a bismuth-free teat seal formulation into the teat canal of the animal. The method also prevents the formation of black spot defect in dairy products, especially cheddar cheese, made from the milk of animals so treated.
EP2549996A1 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(r)-amin0-piperidin-1-yl]-xanthine for the treatment of a metabolic disorder of a predominantly carnivorous non-human animal The present invention provides a pharmaceutical composition comprising 1-[(3-cyano- pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine or a pharmaceutically acceptable form thereof as pharmaceutically active compound for the therapy of a metabolic disorder or metabolic disease of a predominantly carnivorous non-human animal. It is especially useful for the therapy of diabetes and related diseases of predominantly carnivorous mammals like cats or dogs. The invention further provides respective uses of such compositions and of 1-[(3-cyano- pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine or pharmaceutically acceptable forms thereof.
EP1738742A2 Benzyl-1,3-thiazolidine-2,4-dione compounds, compositions comprising them and use for stimulating or inducing the growth of keratinic fibres and/or for diminsihing their loss Use of a benzylidene-1,3-thiazolidine-2,4-dione compound (I) or its salts, solvates and/or cis/trans or Z/E isomers to induce and/or stimulate growth of particularly human keratinous fibers and/or to reduce their fall and/or to increase their density. Use of a benzylidene-1,3-thiazolidine-2,4-dione compound of formula (I) or its salts, solvates and/or cis/trans or Z/E isomers to induce and/or stimulate growth of particularly human keratinous fibers and/or to reduce their fall and/or to increase their density. A1-A4H; A5Z1 group; Z1 : OZ2; Z2 : phenyl (optionally substituted by adamantyl, CF3, halo or 1-20C alkyl); and p : 0-5. Provided that when p is greater than 1, then A5 substituents are identical or different. Independent claims are included for: (1) a care and/or make-up composition for keratinous fibers comprising (I); and (2) a benzylidene-1,3-thiazolidine-2,4-dione compound of formula (I). [Image] - ACTIVITY : Dermatological; Endocrine-Gen. - MECHANISM OF ACTION : 15-hydroxy prostaglandin deshydrogenase inhibitor (15-PGDH). The 15-PGDH inhibiting activity of 5-[3-(4-tert-butylphenoxy)benzyl]- 1,3-thiazolidine-2,4-dione was tested. The results showed that 5-[3-(4-tert-butylphenoxy)benzyl]-1,3-thiazolidine-2,4-dione exhibited an IC50 value of 0.58 mu m.
CN101486689B DPP-IV inhibitor with sulfonamide formamide piperazine structure The invention pertains to the field of medical technology, particularly relating to a DPP-IV inhibitor with a sulfamido formamide piperazine structure shown in the general formula (I), pharmaceutically acceptable salt or an isomer thereof, wherein, R<1>, R<2>, R<3> and Ar are defined as the instruction book; the invention also relates to a preparation method of the compounds, a pharmaceutical composition containing the compounds and applications of the compounds in the preparation of medicaments for treatment and/or prevention of diabetes, noninsulin-dependent diabetes, hyperglycemia, insulinresistance.
EP1140001B1 Composition for treatment of burns The present invention is directed to a composition for treating burns. The composition comprises a therapeutically effective amount of one or more weak organic acid compatible with huamn skin, in a suitable carrier delivered at pH 4.0 - 4.5. The weak organic acid is preferably acetic acid, vinegar, or citric acid and the suitable carrier is preferably an aqueous based carrier, more preferably a gel form, utilizing a CarbopolTM as a gelling agent. The composition may also include one or more other agents selected from sun blocking agents, skin moisturizing agents and herb extracts.
CN103191095A STAT (Signal Transducer And Activator Of Transcription)3 signal channel small-molecule inhibitor and application thereof The invention discloses an STAT (Signal Transducer And Activator Of Transcription)3 signal channel small-molecule inhibitor and application thereof. The inhibitor is expressed in a chemical structural formula which is shown in the specification, wherein R1 is halogenated aryl, R2 is halogenated aryl, R3 is oxygen or sulphur. The inhibitor has functions of effectively inhibiting the multiplication of various tumor cells and inducing the apoptosis of the various tumor cells. The newly developed STAT3 signal channel small-molecule inhibitor not only has a remarkable inhibition effect on the phosphorylation of the STAT3, but also has the remarkable inhibition effect on the IL-6-induced STAT3 activation and the activation of the STAT3 upstream signal CrC and Jak2, and therefore, the multiplication of the various tumor cells can be inhibited and the apoptosis of tumor cells can be induced. Besides, the STAT3 signal channel small-molecule inhibitor has an in-vitro and vivo treatment effect on various tumors of acute and chronic leukemia, multiple myeloma, lymphoma, lung cancer, prostate cancer, cervical cancer and the like.
CN101074189A Styrene acid derivative and use in preparation of various blood-vessels target agent medicine A styrene acid derivative can be used to prepare vascular target agent medicine including antineoplastic medicine and medicine for inhibiting eyeground production. In formula, R1, R2, R3, R4 and R5 are hydrogen, alkyl, hydroxyl, alkoxy, amino, fluorine, chlorine or bromine; R11 is sodium, potassium, lithium, magnesium, calcium or ammonia or organic carboxy-contained ammonium including amino-acid or peptide or glyceryl, hydroxyl, glycosyl containing glucose, multi-hydroxy naphthenic acid containing kinic acid.
CN1765366A Peony total glucosides tablet and its preparation method The invention relates to total glucosides of paeony tablets and the preparing process, which comprises (by weight proportion) 1:0.1-1:10 of total glucosides of paeony raw material and medicinal auxiliary material, wherein the total glucosides of paeony raw material contains 40-100 wt% of glucoside of paeony, each tablet contains total glucosides of paeony 0.1-0.9g, and glucoside of paeony 0.035-0.312g.
US20050032708 up-regulating glutathione metabolism in the central nervous system by up-regulating levels of glutathione precursors (N-acetyl cysteine); for treating neuropsychiatric disorder like schizophrenia, psychosis, bipolar disorder, manic depression, affective disorder, drug induced psychosis, delirium The present invention relates generally to a method of modulating glutathione metabolism in the central nervous system of mammals and to agents for use therein. More particularly, the present invention relates to a method of up-regulating glutathione metabolism in the central nervous system by up-regulating levels of glutathione precursor molecules. The method of the present invention is particularly useful, inter alia, in the treatment and/or prophylaxis of conditions characterised by aberrant, unwanted or otherwise inappropriate central nervous system oxidation homeostasis including, but not limited to, schizophrenia.
US20110038934 Pharmaceutical composition with atorvastatin active ingredient A pharmaceutical composition containing the active substance atorvastatin in the form of oblong-shaped tablets with the length of 5 to 22 mm and the width of 2 to 11 mm or round tablets with the diameter of 3 to 16 mm, the core of which is constituted of compressed granulate and contains: i. Atorvastatin and/or at least one physiologically acceptable salt thereof in the quantity of 5 to 10% by weight, related to pure atorvastatin; ii. An organic or inorganic base selected from meglumine or an alkali metal hydroxide or their combination in the quantity of 0.01 to 7% by weight; iii. A pharmaceutically acceptable filler in the quantity of 20 to 90% by weight; iv. A disintegrant in the quantity of 0.5 to 50% by weight; provided with a coat that makes up 1 to 15% of the weight of the core, the selected base being uniformly distributed in the tablet core by means of spraying the same on the solid mixture in the granule production process. The composition can be obtained by a procedure consisting of the following steps: i. Mixing a mixture of atorvastatin, a filler and a disintegrant; ii. Dissolving a base in a mixture of water and a C1 to C3 alcohol in the quantity of 10:90 to 90:10 (water/alcohol, by weight); iii. Spraying the dry mixture with the base solution either in a masticating or fluidizing device; iv. Adapting the size of particles of the resulting granulate, preferably by re-sieving to the granule size of 0.1 to 1.5 mm; v. Adding other extragranular components to the granulate that will further improve its ability to be compressed into tablets; vi. Compressing the mixture; and vii. Applying a coat on the compressed tablets.
EP2780344A1 Thieno [2, 3 - c]pyrazoles for use as potassium channel inhibitors The present invention provides compounds of formula (I): wherein A, R1, R2, R3 IX, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.
EP2443110A1 S1p1 agonists comprising a bicyclic n-containing ring The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
US20080004300 protein kinase inhibitors such as N-[5-(4,4-Dimethyl-2,5-dioxo-3-pyridin-4-ylmethyl-imidazolidin-1-yl)-2-trifluoromethoxy-phenyl]-2-morpholin-4-yl-acetamide, used for treating tumors; antitumor and anticarcinogenic agents The invention relates to compounds of formula (I): in which R1, R2, L1, X, R3, A, R4, R4′, R4″, R4″′, R5, Y and L2 are as herein defined, salts and prodrugs thereof, to their use as protein kinase inhibitors, and to methods of treating diseases comprising adminstration thereof.
WO2013157889A1 Use of a novel aminopyridine derivative to prevent or treat cancer The present invention relates to the use of a novel aminopyridine derivative to prevent or treat cancer, and more particularly to a carcinostatic composition including a compound of Formula 1 or a derivative thereof as an active principle. The compound of the present invention degrades the activation of AIMP2-DX2 targeted by a novel anticancer drug so as to effectively induce destruction of cancer cells, thus effecting prevention and treatment of cancer. Therefore the compound of the present invention can be used to prevent and treat cancer.
CN103193841A Therapeutic compound and relative usage method A salinomycin analogue and a pharmaceutically acceptable composition containing the salinomycin analogue. The invention comprises a salinomycin analogue, a pharmaceutically acceptable composition containing the salinomycin analogue, and drug forms and kits thereof. The invention also discloses a method for treating proliferative diseases (such as cancer or microbial infection) in subjects by using the salinomycin analogue, the pharmaceutically acceptable composition, and drug forms and kits thereof.
CN101756987A Compound sustained-release preparation of guaiacol olycerin ether, pseudoephedrine and dextromethorphan The invention relates to a sustained-release preparation which takes guaiacol olycerin ether, pseudoephedrine or salt which is physiologically accepted by pseudoephedrine, and dextromethorphan or salt which is physiologically accepted by dextromethorphan as active ingredients. The sustained-release preparation of the invention not only can fully overcome relative symptoms such as cold and express the effect of synergy of compound medicines, but also the release and absorption of three active ingredients of the sustained-release preparation can reach synchronization, and the expected medicine release behavior can be gained inside and outside a human body. The medicine release behavior can reduce the times of taking medicine (from 4 times each day to 2 times each day, i.e. respectively taking medicine once in the morning and in the evening). The preparation is characterized in that times of taking medicine are reduced, the medicine can be slowly released in the human body, the blood concentration is stable, the fluctuation is small, the bioavailability is high, and the safety is high.
CN103239448A Esomeprazole sodium freeze-dried powder composition for injection and preparation method thereof The invention relates to an esomeprazole sodium freeze-dried powder composition for injection and a preparation method thereof. The main medicine of the composition is esomeprazole sodium and L-asparaginic acid. The composition is prepared by the method as follows: (1) weighing water for injection (at 18-20 DEG C) in a proportional liquid container, adding edetate disodium in a prescription amount and stirring to dissolve; weighing 10% sodium hydroxide liquor, adjusting the pH value to 11.5-12.0, and filling high purity nitrogen to the liquor for 5 minutes; (2) then, adding esomeprazole sodium and L-asparaginic acid in a prescription amount, stirring to dissolve, then, adjusting the pH value to 11.6-11.9% by the 10% sodium hydroxide liquor, and then setting the volume to full dose; (3) after adding the main medicine, filling nitrogen to protect the liquid all the way, and maintaining the temperature of the proportional liquid at 18-22 DEG C; weighing 0.1% medicinal carbon, adding a liquid, stirring and adsorbing for 20 minutes, and removing carbon by a 0.45 micron polyether sulfone filter membrane till clarification; (4) filling, introducing nitrogen and arranging a semi-stop; and (5) after freezing and drying, obtaining the esomeprazole sodium freeze-dried powder composition for injection. The composition provided by the invention has the advantages that that the composition is convenient to produce and process, the aseptic operation is simplified, and the quality stability and the compatible stability of products can be ensured at the same time for injections such esomeprazole sodium with higher pH.
EP1628968B1 4-imidazolin-2-one compounds The present invention relates to a compound of the formula [I] wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula [II] wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 may be the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, -NR3R4, -OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.
WO2012034363A1 Compounds of hedgehog pathway inhibitors, pharmaceutical compositions containing the same and uses thereof Compounds of formula I as inhibitors and their process of preparation are disclosed. The compounds can be used to inhibit Hedgehog pathway and can be used as new medicine for treating cancer. Pharmaceutical compositions as inhibitors containing the said compounds which are used as Hedgehog pathway inhibitors for treating cancer are disclosed. The use of said compounds in the manufacture of medicaments of the Hedgehog pathway inhibitors is disclosed.
WO2006123767A1 Method for producing asymmetric tetrasubstituted carbon atom-containing compound Disclosed is a method for commercially producing a spiroaminopyrrolidone derivative as an intermediate for a quinolone antibacterial agent. Specifically disclosed is a method for producing a compound represented by the formula (2) below wherein a compound represented by the formula (1) below is processed in a hydrogen gas atmosphere in the presence of a metal catalyst. (1) (In the formula (1), n represents a number of 2-5; R1 represents a (substituted) alkyl group or a (substituted) aryl group; R2 represents a (substituted) alkoxycarbonyl group, a (substituted) aralkyloxycarbonyl group, a (substituted) aliphatic acyl group or a (substituted) aromatic acyl group; and R3 represents a hydrogen atom, a (substituted) alkyl group or a (substituted) aralkyl group.) (2) (In the formula (2), n, R1 and R2 are as defined above.)
US20080221122 cancer and non-cancer diseases associated with vascular proliferation; mitoxantrone resistant, taxol resistant cancers Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.
EP1637140A1 Use of diphenylmethylpiperazine derivatives for the manufacture of a medicament for suppressing the proliferation of fibroblasts Diphenylmethylpiperazine derivatives which are anticancer agents characterized by being compounds represented by general formula [1], salts thereof, derivatives thereof or prodrugs thereof: [1] wherein R represents (α) or (β). These anticancer agents inhibit the proliferation of fibroblasts, which makes them efficacious against pulmonary fibrosis and proliferative keloid lesion.
US20090062371 Oral preparation for promoting synthesis of tissue collagen An object of the present invention is to provide an oral preparation for promoting synthesis of tissue collagen, an oral preparation for promoting healing of skin wounds or an oral preparation for preventing or improving skin wrinkles or sagging, which is safe and has an excellent effect. The present invention can provide an oral preparation for promoting synthesis of tissue collagen, an oral preparation for promoting healing of skin wounds or an oral preparation for preventing or improving skin wrinkles or sagging, which comprises hydroxyproline or a salt thereof as an active ingredient.
WO2011076732A1 Compounds, pharmaceutical composition and methods for use in treating gastrointestinal disorders The present invention relates to compounds of formula (I) useful in treating and/or preventing gastrointestinal disorders.
CN102885766A Dexketoprofen injection and preparation method thereof The invention discloses a dexketoprofen injection which contains dexketoprofen, an alkaline latent solvent and water for injection, wherein 25g dexketoprofen is contained in the dexketoprofen injection per 1000mL; the molar ratio of the dexketoprofen to the alkaline latent solvent is (1: 0.5)-1.5; and the alkaline latent solvent is alkaline amino acid. In addition, the invention further discloses a preparation method of the injection. In the injection, racemic ketoprofen is replaced by the dexketoprofen, so dosage is little, and side effect is small; and alkaline amino acid is used as a latent solvent, which solves the solubility problem of the dexketoprofen and also overcomes the shortcomings of other latent solvents used in the current preparation; furthermore, the injection can be administered in an intravenous drip way owing to no use of painkiller phenylcarbinol in the injection, thus increasing the medicine administration way; and better safety is ensured because an organic solvent is not used.
CN103027906A Application of arctigenin in treating anemia The invention discloses novel medical application of arctigenin, belonging to the field of medicines. Specifically, the invention discloses a use of arctigenin in preparing a drug for treating anemia. Daily dosage of the arctigenin in treating anemia is preferably 0.1mg/kg.d to 10mg/kg.d. According to the embodiment of the pesticide effect, the arctigenin has a positive effect of treating chronic inflammation anemia, aplastic anemia, hemolytic anemia and renal anemia, therefore, the arctigenin has good clinical application prospect in treating anemia.
EP2780341A1 Kinase modulating compounds, compositions containing the same and use thereof The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.
CN101384264A Therapeutic combinations comprising poly (adp-ribose) polymerases inhibitor The invention generally relates to use of 8-fluoro-2{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one represented by Formula (1) as a chemosensitizer that enhances the efficacy of cytotoxic drugs or radiotherapy. This invention provides pharmaceutical combinations of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, or a pharmaceutically acceptable salt thereof and at least one additional therapeutic agent, kits containing such combinations and methods of using such combinations to treat subjects suffering from diseases such as cancer.
WO2009019518A1 Pyrimidine compounds having a fgfr inhibitory effect There is provided pyrimidine compounds of formula (I): or pharmaceutical salts thereof. There is also provided processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by a FGFR inhibitory effect.
WO2010061877A1 Mineral absorption improver, and method for improving absorption of minerals Disclosed is a mineral absorption improver which has excellent safety and excellent taste, can be ingested for a long period, and can improve the absorption of minerals. The mineral absorption improver comprises an oligosaccharide and a fermented milk product as active ingredients. The mineral absorption improver can improve the absorption of minerals, particularly zinc, by a synergistic effect of the oligosaccharide and the fermented milk product, even though the mineral absorption improver is a composition having a lower oligosaccharide content than those of the conventional mineral absorption improvers. When the mineral absorption improver is prepared using galactooligosaccharide (which is a compound hardly decomposed under acidic conditions) as the oligosaccharide, the mineral absorption improver can be added to compositions such as acidic foods and pharmaceutical preparations.
US20080114004 Hydrazone derivatives as kinase inhibitors The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof as inhibitors of ATP-protein kinase interactions, wherein substituents on each side of the iminomethyl double bond in Formula (I) may be in the E or Z configuration; and wherein R1, R2, R3 and R4 are as defined herein.
US20080139496 Minimising dosage required of chemotherapeutic agents for their use in antiviral, antibacterial, antiparasitic and anticancer chemotherapy; for treating neoplasms and tumours, viral, bacterial, or parasite infections There are provided compositions, pharmaceuticals formulations and kits for treating neoplasms and tumours, viral infections, bacterial infections or parasite infections. There are also provided compositions, pharmaceutical formulations and kits for suppression of immune response rejection in tissue transplantation. Also provided are methods of treating such conditions.
WO2012047918A1 Anti-epileptogenic agents Methods and medicaments therefor are provided for altering an epileptic syndrome in an individual. Methods and medicaments therefor are also provided for preventing an epileptic syndrome in an individual at risk for developing an epileptic syndrome. More specifically, the use of particular glycomimetics for the treatment or prevention is described.
CN101463045B Thiophosphate nucleotide compound The present invention relates to phosphorothioate nucleotide compounds shown in general formula (I) or pharmaceutically acceptable salts or hydrates or solvates thereof which are used as effective antiviral components. The phosphorothioate nucleotide compounds or the pharmaceutically acceptable salts or the hydrates or the solvates thereof have broad-spectrum and high antiviral activity, better safety for an organism and very high oral absorbability.
CN102210676A Antibacterial composite medicine containing sulbenicillin sodium and clavulanic acid compound The invention provides an antibacterial composite medicine containing sulbenicillin sodium and a clavulanic acid compound, a freeze-dried powder injection containing the antibacterial medicinal composition. The medicine consists of sulbenicillin sodium and a clavulanic acid compound, which are in a weight ratio of (2-7):1. Under the same antibacterial condition, the antibacterial composite medicine provided by the invention reduces medicine dose, economic load of patients and production cost.
WO2013079018A1 2-substituted oleanolic acid derivative, method preparing for same, and application thereof The present invention relates to the fields of natural medicaments and pharmaceutical chemistry, and relates specifically to, as represented by formula (I), a novel 2-substituted oleanolic acid derivative or a pharmaceutically acceptable salt thereof, a method for preparing the compounds, a pharmaceutical composition comprising the compounds, and use thereof in preparing an antitumor medicament.
US20110207768 Pharmaceutical combination of antibacterial and antifungal cream A method for the emperic treatment of an intertrigal skin infection potentially caused by a gram-positive bacteria in a human patient that includes a topical administration to the patient of a pharmaceutical formulation comprising a bactericidal amount of a Gram-positive bactericide and an antimycotic amount of an antifungal component suspended in a skin-barrier carrier.
CN101288668A Disinfectant constitutes The invention provides a bactericide, which is mainly used for eliminating the Gram-positive bacteria of Staphylococcus aureus, and Gram-negative bacteria such as colon bacillus, multidrug-resistant Staphylococcus aureus and Propionibacterium acnes. The components thereof contain a solvent and 1 wt percent to 40 wt percent L-ascorbic acid dissolved in the solvent. As Vitamin C is a water-solubility vitamin that can be naturally expelled from the human body even when excessive amount is used, thus the bactericide causes no harm to the human body; in addition, the L-ascorbic acid contained in the bactericide indeed can achieve the effect of inhibiting the proliferation of bacteria and even killing the bacteria. Therefore, the proliferation provided by the invention is completely harmless to the human body.
US20110262534 polysaccharide capsule enclosing a fatty acid oil-containing emulsion Novel capsules where an outer shell comprises a polysaccharide, e.g. an alginate. In the capsules there is an emulsion comprising a fatty acid oil mixture and at least one surfactant. Preferred fatty acid oils are eicosapentaenoic acid (EPA) and doccosahexaenoic acid (DHA).
US20110288080 Nitrofuran Compounds for the Treatment of Cancer and Angiogenesis The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.
US7108845 Methods of synthesis and use of radiolabelled platinum chemotherapeutic agents There is provided a method of synthesis of a radiolabelled platinum chemotherapeutic agent comprising the steps of: converting a metal halide to a radiolabelled platinum halide wherein the radiolabel is a radioisotope of Pt; and synthesizing the radiolabelled platinum chemotherapeutic agent from the radiolabelled platinum halide.
WO2008118091A1 A fumarate salt of 3-bromo-n-{ (2s) -2- (4 -fluorophenyl) -4- [3- (4-acetylpiperazin-l-yl) azetidin-1-yl] butyl} -n-methyl-5- (trifluoromethyl)benzamide for the treatment of gastrointestinal disorders The present invention relates to 3-bromo-N-{(2S)-2-(4-fluorophenyl)-4-[3-(4- acetylpiperazin-1-yl)azetidin-1-yl]butyl}-N-methyl-5-(trifluoromethyl)benzamide fumarate and crystalline forms thereof. The present invention also relates to the use of said salt and crystalline forms thereof for the treatment of gastrointestinal disorders, pharmaceutical compositions containing it as well as processes for the preparation of the salt and novel crystalline forms thereof.
CN102048790A Medical ointment for treating dermatitis and the preparation method thereof The invention relates to a medical ointment for treating dermatitis and the preparation method thereof, which belongs to the technical field of medical skin products. The medical ointment comprises 5-30 parts of Radix Ginseng, 15-30 parts of Herba Epimedii, 5-10 parts of Flos Carthami, 5-20 parts of Margarita, 1-2 parts of Borneolum, 2-5 parts of oxytetracycline tablets and 15-40 parts of vaseline. The medical ointment has the advantages of simple formulation, easily-obtained material, low cost, no toxic and side effects. The medical ointment can treat dermatitis, and has curative effect on bedsore, acne and skin scars. Testified by almost 500 users, the medical ointment has high effective rate (96%), and the preparation method is scientific, reasonable, simple and feasible.
WO2008131502A2 Antiviral compounds of the adamantane type The present invention relates to a series of novel compounds which have been shown to possess antiviral activity, in particular against viruses of the family of the Picornaviridae. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicine, more in particular antiviral medicine.
CN103038219A Compounds acting at multiple prostaglandin receptors to give a general anti-inflammatory response The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula (I). Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.
US8716276 Thiophenyl and pyrrolyl azepines as serotonin 5-HT2C receptor ligands and uses thereof The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thiophenyl and pyrrolyl azepine compounds. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).
US20120322024 Strip for the delivery of oral care compositions Provided herein is a strip, shaped for the application to the labile surface of the front teeth and/or gums of a subject, which strip is provided with at least one oral care composition for delivery to a pre-determined area of the teeth and/or gums of the subject. Also provided herein are uses for delivery of compositions. Further provided are uses of the strip in combination with a dental device.
US7718661 E.g., 4-Difluoro-5-[4-trifluoromethyl-2-(4-trifluoromethyl-phenyl)-imidazo[1,5-a]pyrimidin-8-ylethynyl]-benzenesulfonamide; 4-[4-Difluoromethyl-2-(4-trifluoromethyl-phenyl)-imidazo[1,5-a]pyrimidin-8-ylethynyl]-benzenesulfonamide; metabotropic glutamate receptor antagonists; nervous system disorders The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.
WO2008075528A1 Use of h. macrophylla tea It is intended to develop a novel use of Hydrangea macrophylla var. thunbergii tea. An anti-diabetic composition, which comprises an optionally treated extract of Hydrangea macrophylla var. thunbergii with water, a lower alcohol or a mixture thereof as the active ingredient together with a pharmaceutically acceptable filler or carrier, is provided.
CN103330734A Medium/long-chain fat emulsion injection pharmaceutical composition and preparation method thereof The invention relates to a medium/long-chain fat emulsion injection pharmaceutical composition with improved stability and a preparation method thereof. The composition contains soybean oil for injection, medium-chain triglyceride for injection, lecithin for injection, glycerol for injection, linoleic acid for injection and water for injection. The preparation method comprises the steps of oil phase preparation, water phase preparation, initial emulsion preparation, homogenization, filter membrane filtration, filling, sterilization and the like. In the medium/long-chain fat emulsion injection pharmaceutical composition preparation process, the coemulsifier linoleic acid is added to optimize the preparation technique so as to enhance the emulsifying capacity of the system and reduce and stabilize the emulsion particle size, thereby overcoming the defects of floating oil, enlarged emulsion particle and the like in the prior art; and the invention reduces the number of times of homogenization, enhances the productivity, lowers the methoxyaniline value of the product, and improves the stability and safety of the composition.
WO2008056266A3 Substituted 8-piperidinyl-2-pyridinyl-pyrimido [1,2-a]pyrimidin-6-one and 8-piperidinyl-2-pyrimidinyl-pyrimido[1,2-a]pyrimidin-6-one derivatives The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrirhidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkoxy carbonyl group or a C1-6 alkyl group optionally substituted; n represents 0 to 3; p represents 2; q represents 0; o represents 0, 1 or 2 and m represents respectively 4, 3 or 2, o+m being equal to 4. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.
US20110280859 Preventing and treating sepsis Provided are polypeptides comprising a variant activated protein C comprising one or more amino acid substitutions selected from the group consisting of K146R, D172N, C212R, K146G, R147G, R177G and combinations thereof. Also provided are nucleic acids encoding the polypeptides, and cells, compositions and kits containing the polypeptides and nucleic acids. Also provided are methods of treating sepsis in a subject comprising administering to the subject one or more of the provided polypeptides or nucleic acids. Methods of screening for polypeptides with enhanced activated protein C and for an agent for treatment of sepsis are provided. Finally, provided is a method of treating sepsis in a subject comprising administering to the subject a pharmaceutical composition comprising one or more RGD-containing peptides.
US20120245188 Methods of treating memory loss and enhancing memory performance The present invention provides methods and compositions for enhancing working memory impaired due to aging, Alzheimer's disease, amyotrophic lateral sclerosis (ALS), Parkinson's disease, alcoholism or alcohol withdrawal or Huntington's disease using p38 MAPK inhibitor such as SB239063.
WO2007145253A1 NF-ϰB ACTIVATION INHIBITOR The object is to provide a highly safe NF-ϰB activation inhibitor at a low cost which can be used for the prevention or treatment of a disease associated with the activation of NF-ϰB such as an inflammation or type-2 diabetes. Specifically, the NF-ϰB activation inhibitor comprises a compound represented by the chemical structural formula depicted in Chemical Formula 1 [wherein R1 represents a hydroxy group; R2 represents a hydroxy group, a methoxy group or an alkoxy group; and R3 represents an ester comprising a triterpene or a salt thereof] or a salt of the compound as an active ingredient. Arepresentative example of the compound is a hydroxycinnamic acid derivative triterpene alcohol ester.
CN1989975A Method for preparing composite injection of 12 vitamins The invention discloses a process for preparing compound injection of 12 kinds of vitamins, which comprises steps of mixing water soluble vitamins, fat soluble vitamins, solubilizing agent, auxiliary solvent, solvent and water for injection, stirring into colloidal solution state, charging activated charcoal for adsorbing, finally adjusting pH of the solution.
CN103110650A Application of astragalin in preparation of anti-ovarian-senescence medicaments The invention discloses the application of astragalin in preparation of anti-ovarian-senescence medicaments. Astragalin can treat various ovarian failure diseases, and has a remarkable effect on polycystic ovarian syndrome, dysfunctional uterine bleeding, premature ovarian failure or climacteric syndrome and the like. According to the invention, astragalin is prepared into oral medicaments, percutaneous medicaments or parenteral medicaments for treating ovarian failure diseases.
US20090029935 Centrosomal proteins and secretion Described are methods for modulating cellular secretion, and methods for identifying novel modulators of cellular secretion, that target centrosomal proteins.
CN101033226B 1-furylmethyl-3-substituted indolin-2-one derivative This invention relates to a derivant of 1-furan methyl-3-replaced indole-2-ketone derivant especially to indole-2-ketone derivant replaced by 1-(5 replaced furan methyl) indole-2-ketone compound in three bits, its preparation method and the application on medicine. This invented compound has fine anti-cancer activation compared with anode contrast to anti-cancer medicine.
CN101036635A Compound diisopropylamine dichloroacetate sodium chloride injecta The invention provides a compound dichloroacetic acid diisopropylamine sodium chloride injecta and a method for preparing the same. The product has main components of dichloroacetic acid diisopropylamine, sodium gluconate and sodium chloride which proportion of each component is in that: dichloroacetic acid diisopropylamine : sodium gluconate : sodium chloride = 15-16 : 1050 : 2000. The preparing method is in that: the dichloroacetic acid diisopropylamine, sodium gluconate and sodium chloride are used according to a prescription quantity and dissolved by water for injection in 70% prescription quantity, adding 0.15% active carbon, heat preservating and adsorbing in 15-30 minutes at 50-70 DEG C, filtering, adding water for injection to total quantity, PH value is controlled to 4.0-6.0 by chlorhydric acid, fine filtering by 0.22 mu m filtration membrane, detecting, canning, sterilizing for 15-30 minutes at 100-200 DEG C, sealing and packaging. The invention simplifies processes of traditional temporary dispensation, prevents pollution, facilitates to use the medicine, and improves the efficiency. The product is applicable to treating oxyhepatitis and chronic hepatitis.
US20110200675 Drug delivery vehicles, methods of manufacture, and methods of use thereof Drug delivery vehicles that release one or more drugs, e.g., an opioid antagonist and/or an opioid, in response to changes in the chemistry of body fluids, specifically in response to changes in the partial pressure of CO2 in the environment of the hydrogel are described. The drug delivery vehicles include hydrogels that swell or shrink in response to changes in the partial pressure of CO2 in their environment, thus regulating release of an entrapped drug.
US20100240612 Prenylated Bisphosphonates as Anti-tuberculosis Agents The invention provides methods to treat a mycobacterium infection and methods to inhibit mycobacterial polyprenyl pyrophosphate synthesis with a compound of formula I. The invention also provides novel compounds of formula I as well as salts and prodrugs thereof.
CN1931869B Derivative of 5-deoxy-5-fluoro cytidine and its preparation process and use The present invention relates to a compound of the general formula (I) and medicinal salt thereof, wherein R1 and R2 are independently selected from hydrogen, C[1-6] straight-chain or branched-chain alkyl, phenyl and phenyl optionally substituted by C[1-6] alkyl or C[1-6] alkoxy; the condition is that at least one group in the R1 and R2 is not hydrogen; X represents O or S; R3 is selected from hydrogen, C[1-6] straight-chain or branched-chain alkyl, phenyl and phenyl optionally substituted by C[1-6] alkyl or C[1-6] alkoxy; R4 and R5 are independently selected from hydrogen or two (C[1-6]) alkyl amido, the condition is that at least one group in the R4 and R5 is not hydrogen; or R4 and R5 can be combined into a ring and form N-substituted pyrrolidinyl or N-substituted piperdine, and the substituted group is selected from C[1-3] alkyl. The present invention also relates to a preparation process of the compound. The present invention further relates to a medicine composition containing the compound or its medicinal salt and the application of the compound or its medicinal salt in preparation of antitumor medicine.
WO2012146933A1 Cyprodinil for use in medicine There is provided anilinopyrimidine compounds (such as Cyprodinil) for use in medicine, preferably for the treatment of cancer.
WO2010101888A3 Methods and compositions for treatment of tumor metastasis The various embodiments of the present invention are directed to methods and compositions for treatment, inhibition, or reduction of metastasis in cancers. In particular, the invention is related to compositions and methods affecting connective tissue growth factor (CTGF). An aspect of the present invention comprises a method for interfering with the activity of connective tissue growth factor, comprising, administering to a subject an effective amount of a composition that inhibits production of or activity of connective tissue growth factor (CTGF), wherein the composition interferes with the activity of CTGF or prevents the transcription of CTGF genes or translation of CTGF mRNA. For example, the composition can comprises at least one HMG-CoA reductase inhibitor compound, such as a statin.
US20120180147 Microrna-24 The present invention relates to a modulator, in particular an inhibitor, of microRNA-24 (miR-24) and to direct and indirect miR-24 targets for use in a method of treatment and/or prevention of ischemia, in a method of prevention of endothelial apoptosis or in a method of induction of angiogenesis. The present invention further relates to a precursor of miR-24 and to siRNAs or shRNAs against direct or indirect miR-24 targets for use in a method of treatment of angiogenesis associated with cancer. The present invention also relates to an in vitro method for diagnosing ischemia or prevalence or disposition for ischemia, and to a method for identifying a modulator of miR-24 and/or direct or indirect miR-24 targets. In addition, the present invention relates to pharmaceutical compositions or kits comprising any of the above agents, to endothelial cells devoid of expressing functional miR-24, and to a non-human, transgenic animal comprising these endothelial cells.
WO2007116029A2 Combination comprising a) a pyrimidylaminobenzamide compound, and b) a thr315lle kinase inhibitor The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) a Thr315lle kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.
WO2014062960A1 Treatment and prevention of mastitis Treating and Preventing mastitis employing cationic steroidal antimicrobials (CSAs). Treating or preventing clinical mastitis in a mammal includes administering a cationic steroidal anti-microbial compound (CSA) formulation to the intra-mammary organ of a mammal (e.g., a dairy cow), such as by injection into the mammary organ (e.g., through the teat of the mammary organ), and/or topical application. The dairy cow can be lactating and have a somatic cell count (SCC) less than or equal to 500,000 cells/mL at the time of administering the CSA formulation. Alternatively, the dairy cow can be lactating and have a somatic cell count (SCC) greater than 500,000 cells/mL at the time of administering the CSA formulation. The dairy cow can be taken out of production during the administration of the CSA formulation for a period of time of about 3 days or less, 2 days or less, or 1 day or less.
US20090036475 Pyrazolyl-Pyrimidines as Potassium Channel Modulating Agents and Their Medical Use This invention relates to novel potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, in particular respiratory diseases, epilepsy, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic heart disease, angina pectoris, coronary heart disease, traumatic brain injury, psychosis, schizophrenia, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labour, baldness, cancer, immune suppression or pain.
WO2012040623A2 Nanostructured gels capable of controlled release of encapsulated agents Self-assembled gel compositions including a gelator, e.g., an enzyme-cleavable gelator, e.g., having a molecular weight of 2500 or less, are described. The self-assembled gel compositions can encapsulate one or more agents. Methods of making the self-assembled gel compositions, and methods of drug delivery using the self-assembled gel compositions are also described.
EP2303231A1 Preparation containing glucosamine and/or chondroitin for prophylaxis and treatment of arthrosis and for supporting the immune system The present invention describes a liquid, aqueous formulation comprising: 1 to 60 wt.-% of a component (a) that consists of glucosamine and/or a physiologically acceptable derivative of glucosamine and/or chondroitin and/or a physiologically acceptable derivative of chondroitin, 0.1 to 30 wt.-% of a component (b) that consists of a phospholipid and/or a physiologically acceptable derivative of a phospholipid and 5 to 90 wt.-% of a component (c) consisting of a micelle stabilizer selected from the group consisting of (c1 ) carnitine and/or a physiologically compatible carnitine derivative, and (c2) one or more polyol(s) selected from the group consisting of: aldoses, ketoses, reduced aldoses and/or ketoses, physiologically acceptable glycosides of aldoses and/or ketoses, C3-C6- triols, C3-C6- tetraols, C3-C6- pentanols and C3-C6 hexanols, wherein each of the weight amounts relates to the total formulation.
US20120015895 Use Of RR/SR-Ractopamine A method of promoting or improving the feed efficiency and the muscle-to-fat ratio in animals by administering to the animals a therapeutically effective amount of a mixture of RR-ractopamine and SR-ractopamine is disclosed. Manufacturing methods for making RR/SR-ractopamine are presented.
US20100287637 Methods of blocking tissue destruction by autoreactive t cells Methods for blocking autoreactive T cell-initiated destruction of tissues in a mammal are provided. In one embodiment, the method comprises administering a purified CD24 polypeptide, a fusion protein comprising such polypeptide, or a biologically active fragment of such polypeptide to a mammalian subject who is suspected of having or predisposed to having an autoimmune disease. In another embodiment, anti-CD24 antibody or anti-CD24 Fab fragments are administered to the subject. In another embodiment, the method comprises administering a CD24 antisense molecule, an expression vector encoding a CD24 antisense molecule, CD24 dsRNAi, or an expression vector encoding CD24 dsRNAi to the subject. The present invention also relates to isolated and purified CD24 fusion proteins employed in the present methods and to transgenic mice that express the human CD24 protein on their T cells and/or their vascular endothelial cells but do not express murine heat shock antigen on any cells.
US20120289469 Methods and compositions for maintaining active agents in intra-articular spaces Methods and compositions for maintaining an active agent in an intra-articular space are disclosed. Methods of delivering the compositions to an intra-articular space and methods of making the compositions also are disclosed. The compositions comprise an active agent and a polymer comprising at least one cationic group. A fluid including the composition may be injected into an intra-articular space in a human or animal whereby the composition associates with endogenous material in the intra-articular space. In some embodiments, the fluid further comprises a poorly aqueous soluble polymer.
WO2009041456A1 Imidazopyridazine derivative Disclosed is a novel low-molecular-weight compound which has an inhibitory activity on the production of TNF-α, which is useful as a therapeutic agent for an inflammatory disease and/or an autoimmune disease, and which can be administered through an oral route. Specifically disclosed is a compound represented by the general formula (I), a salt thereof, or a solvate of the compound or the salt. (I) wherein R1 represents a group represented by the formula alkylene-X1-X2; X1 represents a single bond or the like; X2 represents a C1-C6 alkyl group; R2 represents a hydrogen atom or the like; R3 represents a group represented by the formula alkylene-Y; Y represents an amino group or the like; R4 represents a group represented by the formula Z1-Z2; Z1 represents an alkylene group or a group represented by the formula alkylene-O-alkylene; and Z2 represents an amino group or the like.
CN102526291A Health care product used for alleviating dysmenorrhea The invention discloses a health care product used for alleviating dysmenorrhea, which is prepared from the following raw materials in parts by weight: pericarpium citri reticulatae, spina date seed, rhizoma corydalis, borneol, astragalus polysaccharide, angelica sinensis polysaccharide, leonurus polysaccharide, rehmannia polysaccharide, allicin, vitamin D, vitamin E and oyster calcium. The health care product used for alleviating dysmenorrhea has the efficacy on effectively regulating menstruation, killing pain and controlling the dysmenorrhea, has a small toxic and side effect and is safe to use.
CN103083285A Oral mucosa medicine slow-release preparation for treating oral and periodontal diseases by using tetracycline The invention relates to the field of medicines for treating oral mucosa diseases and preparation thereof, in particular to an oral mucosa medicine slow-release preparation for treating oral and periodontal diseases by using tetracycline. The preparation consists of an oral mucosa contact layer and a non-adhesive closing layer, wherein the oral mucosa contact layer comprises antibiotic medicines and accessories in a weight ratio of (2-20):(80-98); the non-adhesive closing layer comprises non-adhesive low water-soluble macromolecular polymer; the non-adhesive low water-soluble macromolecular polymer is polyvinyl alcohol; and the oral mucosa medicine slow-release preparation comprises 17.6 grams of ethyl hydroxyethyl cellulose, 9.8 grams of hydroxymethyl starch, 0.6 gram of strawberry essence, 4.0 grams of tetracycline, and the balance of polyvinyl alcohol. The oral mucosa medicine slow-release preparation has the advantages of convenience in application, long medicine release time, uniform medicine release speed, strong targeting property, strong adhesion with mucosa and the like; and a preparation method is easy to operate, low in cost, environment-friendly and suitable for industrialized production.
US20120053196 Combination Treatment of Breast Cancer The present disclosure provides products including an endocrine treatment product and a statin as a combined preparation for simultaneous, separate or sequential use in therapy. Further, there is provided a method of treatment of a mammalian breast cancer subject, comprising simultaneous, separate or sequential administration of therapeutically effective amounts of a statin and an endocrine treatment product.
US20120114762 Physico-Chemical-Managed Killing of Penicillin-Resistant Static and Growing Gram-Positive and Gram-Negative Vegetative Bacteria Systems and methods for the use of compounds from the Hofmeister series coupled with specific pH and temperature to provide rapid physico-chemical-managed killing of penicillin-resistant static and growing Gram-positive and Gram-negative vegetative bacteria. The systems and methods represent the more general physico-chemical enhancement of susceptibility for a wide range of pathological macromolecular targets to clinical management by establishing the reactivity of those targets to topically applied drugs or anti-toxins.
US20070259045 Alcohol Resistant Dosage Forms Disclosed in certain embodiments is a controlled release dosage form comprising a matrix comprising a pharmaceutically acceptable salt of an opioid analgesic in a controlled release material; wherein less than 25% of the opioid salt is released after 1 hour of in-vitro dissolution of the dosage form in 900 ml of Simulated Gastric Fluid with 20% ethanol using a USP Apparatus I (basket) apparatus at 100 rpm at 37 degrees C.°.
US20050014788 Piperidine derivatives and their use as modulators of chemokine receptor activity (especially ccr5) Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
CN101991549A Antipyretic, analgesic and anti-inflammatory medicinal composition The invention relates to an antipyretic, analgesic and anti-inflammatory medicinal composition injection, wherein a molar ratio of arginine to ibuprofen is 1.01:1-1.5:1, and in particular provides a method for preparing the composition injection. The injection contains an injection subjected to high temperature sterilization and a freeze-dried powder injection subjected to low temperature freeze drying. The composition is simple in preparation and easy to control and can greatly improve the stability of composition aqueous solution, improve the bioavailability of the medicament, reduce the response time of the medicament and gain more valuable time for the treatment of patients.
US20100317639 Medicament Based On a Monoester of Steroids With Long Chain Fatty Acids A monoester of a family of steroids with a C16-C24 fatty acid for use as a medicament is disclosed. Particularly the monoester of 5α-androstan-3α,17β-diol with a C16-C24 fatty acid is disclosed, such as preferably linoleic acid in all its isomeric forms. The medicament is capable to reduce the accumulation of cholesterol esters, reducing the ACAT enzyme (acyl-coenzyme A: cholesterol acetyltransferase) effect so that monoesters are used for the manufacture of a medicament for treating adrenoleucodistrophy, Alzheimer's disease and arteriosclerosis.
CN102485229A Antiviral medicine The invention relates to an antiviral medicine, and specifically relates to crystals of an acyclic nucleotide analogue represented by a formula I. the crystals can be crystals of free alkali of the acyclic nucleotide analogue represented by the formula I, and can be crystals of a composition of the acyclic nucleotide analogue represented by the formula I and salts formed by various inorganic acids or organic acids. The characteristics of the crystals can be determined by X-ray powder diffraction analysis spectra and melting points.
CN103356738A Skin disinfection gel and its application Belonging to the technical field of disinfection, the invention discloses a skin disinfection gel to solve the disadvantages of existing disinfection technologies, especially preoperative disinfection technologies. The skin disinfection gel is composed of the following active components by mass: 1.5%-6% of chitosan, 1.5-10% of chitosan oligosaccharide, 2%-8% of baicalin, 0.5%-2% of chlorhexidine, 0.5%-1.5% of sodium alginate, 2%-5% of agarose, and 1.5%-5% of a mint extract. And the disinfection effect is good. The disinfection gel disclosed in the invention can be used for hand disinfection or skin disinfection in sanitary disinfection or preoperative disinfection, and with excellent disinfection effects and lasting function, it has very good application prospects and economic benefits.
US7879893 Zinc binding ligand; sustained release of insulin The present invention relates to novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer having the formula A-B-C-D-X (III), wherein: A is a chemical group which reversibly binds to a HisB10 Zn2+ sites of an insulin hexamer; B is a linker; C is a fragment consisting of 0 to 5 neutral amino acids; D is a fragment comprising 1 to 20 positively charged groups independently selected from amino or guanidino groups; and X is —OH, —NH2 or a diamino group. The present invention also relates to R-state insulin hexamers comprising such ligands, and aqueous insulin preparations comprising such R-state insulin hexamers.
US8853202 Modulators of CXCR7 Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.
CN101519372A Benzo [e] isoindazole-1,3 diketone compound used as GSK inhibiting agent and preparation method thereof The invention provides a multiring structure diketone micromolecule compound and a preparation method thereof. Compared with the existing GSK 3 inhibiting agent, the compound has the characteristics of small molecule, simple structure, easy synchronization, and the like, better inhibits the activity of GSK 3, and can be used for researching and developing medicines adopting GSK 3 as a drone. The invention also provides derivant based on the micromolecule compound, which also has the function of inhibiting the activity of GSK 3.
CN101259140B Compound medicaments treating gastritis, gastric ulcer, and duodenal ulcer and preparation thereof The present invention provides a compound medicine or capsule for remedying the gastritis, the gastric ulcer and the duodenum ulcer, which mainly contains glutamine, the coprecipitator of aluminium hydroxide and sodium bicarbonate, ethanol piperidine hydrochloride and medical accessory materials. The mix radio by weight of each component are 200 to 300 portions of the glutamine, 60 to 100 portions of the coprecipitator of aluminium hydroxide and the sodium bicarbonate, 1 to 1.5 portions of the ethanol piperidine hydrochloride, 0 to 30 portions of filling agent, 1 to 10 portions of wetting agent, 0 to 10 portions of bond, 0 to 10 portions of disintegrant and 0 to 2 portions of lubricant. The prevent invention makes up the disadvantage of the single therapeutic action of the prior medicine for remedying the gastritis, the gastric ulcer and the duodenum ulcer and provides a compound medicine which has more comprehensive therapeutic actions of relieving hyperacidity, spasmolysis and restoring damaged gastrointestinal mucosal for the gastritis, the gastric ulcer and the duodenum ulcer. At the same time, the present invention provides the preparation method of a compound glutamine tablet and capsule.
CN102038811A Rapid ecthyma healing plaster The invention provides a formula and a production process of a rapid ecthyma healing plaster for treating ecthyma. The rapid ecthyma healing plaster mainly comprises angelica sinensis tail, calamine, calcined keel, red halloysite, amber, nacre, dragon's blood, herba orostachyos, elephant hide, borneol, human placenta, cera chinensis and sesame oil, and is characterized by having the effects of clearing heat and detoxifying, removing decay and eliminating dampness, activating blood and dissolving stasis, activating meridians and relieving pain, emphasizing tonifying, and rapidly astringing ecthyma and promoting tissue regeneration. The rapid ecthyma healing plaster has the advantages of simple process, no toxic and side effects, rapid curative effect and low cost, is easily accepted by the patients and is worthy of popularization; and the drug sources of rapid ecthyma healing plaster are wide.
US20080262023 Aminomethyl Azaadamantane Derivatives and Methods of Use Thereof The invention relates to compounds that are substituted aminomethyl azaadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
EP1814532A2 Topical application of muscarinic and opioid agents for treatment of tinnitus The present invention relates to a composition and methods for treating tinnitus. In preferred embodiments of the invention, muscurinic and/or opioid agents are administered to the affected ear in amount effective to relieve one or more tinnitus symptoms. A preferred agent is an anticholinesterase inhibitor, such as neoostigmine.
CN102846637A Veterinary drug for treating dysbacteriosis of chicken The invention discloses a veterinary drug for treating dysbacteriosis of chicken, and is characterized in that the veterinary drug comprises enrofloxain hydrochloride, moroxydine hydrochloride, aspirin, vitamin A, vitamin E, vitamin C and glucose. The inventive veterinary drug can effectively treat dysbacteriosis of chicken, has evident curative effect and convenient application, and deserves wide generalization.
WO2009031943A1 Method for monitoring diabetes insulin therapy The invention relates to medicine, in particular to endocrinology, more specifically to the monitoring of insulin therapy of patients suffering from diabetes. The method for monitoring diabetes insulin therapy is based on the measurement of a glucose concentration in the blood or in the hypodermic medium by means of an optical and/or electrochemical method, and consists in periodically injecting test doses of (ultra) short insulin into a measuring point, thereby generating a short-term local deterioration of a glucose level and obtaining a difference in measurement results for determining a current glucose level during a given measuring interval. The inventive method makes it possible to increase the accuracy of measurement of a current glycemia level, also when using a non-invasive method of measurement, since the result depends only on two parameters, i.e. the insulin test dose and the current glucose level in the organism.
CN101675917A Propofol self-micro-emulsifying composition and preparation method thereof The invention relates to a propofol self-micro-emulsifying composition and a preparation method thereof, mainly aiming at solving the technical problems of injection pain and extremely low oral bioavailability of the existing fat emulsion. The invention has the technical scheme that the propofol self-micro-emulsifying composition comprises the components by weight percent: 1-15% of propofol, 10-70% of emulsifying agent, 0-50% of auxiliary emulsifying agent and 0-30% of oil phase. The new formulation of propofol has the characteristics of low gastrointestinal metabolism, higher bioavailability,good stability and easy preparation.
US7211590 Such as 2-(nitrooxy)ethyl-2-(((3-methyl-4-(2,2,2-trifluoro-ethoxy)-2 -pyridyl)methyl)sulfinyl)benzimidazolecarboxylate; kits; for treating gastrointestinal disorders/ulcers The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated proton pump inhibitor compound, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti-Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.
CN101940565A Application of T-2 toxin in preparing drug for treating prostatic cancer The invention discloses novel application of a T-2 toxin, in particular to application of the T-2 toxin in preparing a drug for treating prostatic cancer. The effective curative dose of the T-2 toxin is 0.1-20mg per kg of body weight, preferably 0.5-8mg per kg of body weight. When in administration, implantation administration, oral administration, intravenous injection administration, hypodermic injection administration and intramuscular injection administration can be adopted, preferably intratumoral injection. The inventor of the invention establishes various hypostatic tumor models and then inspects the inhibitory action of the T-2 toxin on tumor or tumor cells through a mode of carrying out the intratumoral injection or cell coculture on the T-2 toxin. Proved by an experiment, the intratumoral injection has the exact curative effect on the tumor, in particular to the hypostatic tumor which is difficult to cut off, and moreover, through the administration by the intratumoral injection, the side effect range and degree of the T-2 toxin can be further reduced, the side effect of the T-2 toxin is reduced whereas the inhibitory action and the killing action of the T-2 toxin are enhanced.
EP1525209A2 1'-, 2'- and 3' -modified nucleoside derivatives for treating flaviviridae infections 2' and 3'-Prodrugs of l', 2', 3' or 4'-branched ß-D or ß-L nucleosides, or their pharmaceutically acceptable salts and derivatives are described, which are useful in the prevention and treatment of Flaviviridae infections and other related conditions. These modified nucleosides provide superior results against flaviviruses and pestiviruses, including hepatitis C virus and viruses generally that replicate through an RNA dependent RNA reverse transcriptase. Compounds, compositions, methods and uses are provided for the treatment of Flaviviridae infection, including HCV infection, that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.
US20100292197 Compositions and Methods for Increasing Telomerase Activity The present invention relates to methods and compositions for increasing telomerase activity in cells. Such compositions include pharmaceutical formulations. The methods and compositions are useful for treating diseases subject to treatment by an increase in telomerase activity in cells or tissue of a patient. They are also useful for enhancing replicative capacity of cells in culture, as in ex vivo cell therapy and for enhancing proliferation of stem and progenitor cells.
US20080214661 Process To Obtain Dibenzylbutyrolactonic, Tetrahydrofuranic Lignans And Their Synthetic And Semi-Synthetic Derivatives, Their Analgesic And Anti-Inflammatory Activities, Topical And/Or Systemic Formulations Containing Said Lignans And Their Respective Therapeutic Method A process to obtain dibenzylbutyrolactonic lignans from (-)-cubebin, isolated from a Piperaceae, especially Piper cubeba, and from (-)-methylpluviatolide, isolated from a Rutacea, especially Zanthoxylum naranjillo; their synthetic and semi-synthetic derivatives and tetrahydrofuranic lignans, such as galgravin and veragensin, isolated from Nectandra megapotamica, as well as the analgesic and anti-inflammatory activities of said lignans, and the topical and/or systemic formulations. Also presented is a therapeutic method using topic and/or systemic formulations based on said lignans for the treatment of inflammation and/or pain. Further, a process to obtain synthetic and semi-synthetic derivatives of (-)-cubebin, such as: (-)—O-acetyl cubebin; (-)—O-methyl cubebin; (-)—O—(N,N-dimethylamino-ethyl)-cubebin; (-)-hinokinin; (-)-6,6′-dinitroinokinin; (-)—O-benzyl cubebin; (-)-6,6′-diaminohinokinin and other synthetic derivatives which may be obtained, and synthetic and semi-synthetic derivatives of (-)-methylpluviatolide, such as (-)-6,6′-dinitromethylpluviatolide and (-)-6,6′-diaminomethylpluviatolide, to be used in the manufacture of medicine that has analgesic and anti-inflammatory activity is presented.
US20100048504 Crystalline and amorphous forms of beta-l-deoxythymidine Physical forms of beta-L-2′-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2′-deoxythymidine can be used in the manufacture of other forms of beta-L-2′-deoxythymidine, or in pharmaceutical compositions. Particularly preferred uses are in the treatment of hepatitis B.
WO2014100417A1 Compounds, compositions, and methods for the treatment of cancers The present teachings relate to compounds and compositions for treatment of cancers. In some embodiments, the composition comprises a platinum (IV) complex having at least one carboxylate or carbamate ligand.
CN201216753Y Dressings emplastrum for relieving pain of tumour The utility model discloses an adhesive plaster for relieving pain caused by tumor. The technical proposal adopted by the utility model is as follows: the adhesive plaster for relieving pain caused by tumor comprises an adhesive bottom flake, a dressing block and an ointment, and is characterized in that the ointment (3) is immersed in the sterile dressing block (2); the dressing block (2) is fixed in the middle position of the adhesive bottom flake (1); and after being fixed, the adhesive bottom flake is loaded into a plastic-film, vacuum, moisture-holding and sealed bag. The technical proposal comprises the following steps: folding a medicinal gauze into a multi-layer square (six by six centimeter) dressing block (2); placing the ready-made ointment (3) in a stainless steel dressing container for sterilization and disinfection through dry-heating; then placing the sterile dressing block (2) uniformly into the container to allow the ointment to immerge into the block; selecting the adhesive bottom flake (1) (eight by eight centimeter); placing the dressing block (2) with the well-immersed ointment (3) in the middle position of the adhesive bottom flake (1); and loading the fixed adhesive bottom flake into the plastic-film, vacuum, moisture-holding and sealed bag.
EP0651805B1 Method of intracellular binding of target molecules The present invention relates to a method by which one can target an undesired target molecule or target antigen, preferably a protein. The method comprises the intracellular expression of an antibody capable of binding to the target. A DNA sequence is delivered to a cell, the DNA sequence contains a sufficient number of nucleotides coding for the portion of an antibody capable of binding to the target operably linked to a promoter that will permit expression of the antibody in the cell(s) of interest. The antibody is then expressed intracellularly and binds to the target, thereby disrupting the target from its normal actions.
US7649080 Reacting vancomycin with a coupling reagent, then reacting with a cephalosporin derivative; making antibiotic effective against antibiotic-resistant strains of bacteria, such as methicillin-resistant Staphylococci aureus (MRSA) This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.
EP1181001B1 Sunscreen composition containing sol-gel microcapsules The present invention generally relates to safe and stable sunscreen compositions comprising at least one sunscreen active ingredient in the form of an inert sol-gel microcapsules encapsulating ultraviolet absorbing compounds in any acceptable cosmetic vehicle. The composition according to the present invention can comprise several ultraviolet absorbers that may be encapsulated in the same sol-gel microcapsule or in different capsules. The encapsulation of the ultraviolet absorbers reduces or even prevents the contact between the sunscreen compounds and the human tissue, thus reducing various adverse effects that are associated with the use of sunscreens. The encapsulation also reduces or even prevents cross reactivity between the suscreen compounds and the packaging material and between the suscreen compounds and any other component present in the composition, thus enhancing the compositions stability. The hydophobicity/hydrophilicity character of the sol-gel microcapsules can be controlled by selecting suitable sol-gel precursors and suitable reaction conditions and can be chosen to be compatible with the cosmetic vehicle to be used in the sunscreen composition. The sunscreen compositions of the present invention can comprise any acceptable UVA and/or UVB absorbing compounds at any desired ratio to obtain a desired accumulative ultraviolet screening spectrum.
CN103263431A Application of polyflavanostilbene A in preparation of medicaments for treating tongue carcinoma The invention discloses an application of polyflavanostilbene A in preparation of medicaments for treating tongue carcinoma, belonging to the technical field of new uses of the medicaments. The invention finds that the polyflavanostilbene A also has a significant inhibition effect against the growth of human tongue carcinoma cell strains PTca8113 and T6 through in-vitro MTT anti-tumor activity evaluation. Therefore, the polyflavanostilbene A can be used for preparing anti-tongue carcinoma medicaments and further has good development and application prospects. The use of the polyflavanostilbene A in the preparation of the medicaments for treating the tongue carcinoma, disclosed by the invention, belongs to the first disclosure, and the strong inhibition activity against cells of the tongue carcinoma is further unexpected.
CN101633652B Baicalein-8-sodium sulfonate and preparation method thereof and pharmaceutical use thereof The invention belongs to the technical field of a heterocyclic compound, in particular to the heterocyclic compound which contains a heterocyclic non-hydrogenated six-membered ring, and takes an oxygen atom as the only heterocyclic atom to connect with a benzene ring and a fused aromatic ring at a position 2. The invention provides baicalein-8-sodium sulfonate and a preparation method thereof, and the process comprises the following steps: adding a reactant baicalein and a sulfonating agent into solvent, allowing the reactant to chemically react with the sulfonating agent to obtain the mixture of the compound in the invention and unreacted reactants, and purifying the mixture by a conventional separation method to obtain the purified product of the compound. The invention further provides an anti-aging medicine and composition, the baicalein-8-sodium sulfonate with therapeutically effective amount, a pharmaceutically acceptable carrier, and application of the baicalein-8-sodium sulfonate in preparing the anti-aging medicine.
CN101002731A Wound-protection liquid, and its preparing method A wound nursing liquid for controlling infection and promoting healing of wound contains proportionally Ag ion powder, gelatin, binary acid, penetrant, tartaric acid and purified water. Its preparing process is also disclosed.
CN1919846A Novel oriented synthesis method of voriconazole, medicinal salt and intermediate thereof The invention discloses a new-typed antibiotic drug and medical salt and preparing method of one new directional intermediate, which is characterized by the following: adopting directional ketone synthetic technology corresponding to metal organic compound; preparing key intermediate (2R,3S/2S,3R)-2-(2,4 difluorobenzene-3-(4-chlorin-5-fluoxydin-6-radical)-1-(1H-1, 2, 4-ribavirin-1-radical)-2-butanol or salt; reducing; dechlorinating; detaching to obtain voltyokonoside.
CN101983706A External used medicine paste for treating various bone hyperplasias and preparation method thereof The invention discloses an externally-used medicine paste for treating various bone hyperplasias. The medicine paste is mainly prepared by notopterygium root, radix angelicae pubescentis, frankincense, myrrh, safflower, large leaf gentian root and rhizoma ligustici wallichii in certain weight proportion. The invention has the effects of promoting blood circulation and removing blood stasis, activating collaterals, eliminating dampness and expelling the wind as well as setting fractured tendons and bones, curative effect on bone hyperplasia is quick, and curative ratio is high.
WO2005072750A1 Composition for inhibting dietary lipid absorption It is intended to provide a composition having an excellent effect of inhibiting lipid absorption which can inhibit the absorption of lipids taken by meals and contribute to the efficient discharge of the lipids from the body. This composition is characterized by containing (1) chitosan and (2) at least one water-soluble dietary fiber selected from the group consisting of guar gum, pectin, tara gum and locust bean gum.
WO2011073263A1 1, 7 - diazacarbazoles and their use in the treatment of cancer The invention relates to 1, 7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk 1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
CN102716081B Docetaxel vesicle type phospholipid gel injection The invention discloses docetaxel vesicle type phospholipid gel injection and a preparation method of the docetaxel vesicle type phospholipid gel injection. The docetaxel vesicle type phospholipid gel injection is prepared from docetaxel, phospholipid, cholesterol and freeze-drying supporting agents according to a specific weight ratio. The docetaxel vesicle type phospholipid gel injection has good preparation stability, the clinical use is convenient, and the vesicle type phospholipid gel maintains good encapsulation rate after long-period storage. The docetaxel vesicle type phospholipid gel injection and the preparation method have the advantages that the quality of the preparation product is improved, the bioavailability of the medicine is improved, the toxic and side effects are reduced, and in addition, the preparation method is simple and is suitable for industrial mass production.
EP1554586B1 Identification of drugs against mycobacteria The present invention relates to a package of screening methods for developing drugs against pathogenic microbes having two-component system of DevR-DevS and/or DevR-Rv2027c and its homologues, said method comprising steps of over-expressing DevR, DevS, and Rv2027c and their single domain derivatives including mutant variant proteins, autophosphorylating DevS, and Rv2027c proteins and thereafter, phosphotransfering to DevR and its derivatives in SDS-PAGE or High-throughput format in the presence of a test compound, and determining the drug-potential of the test compound, wherein the potential of the drug is inversely proportional to (i) the degree of autophosphorylation of DevS and Rv2027c, (ii). the degree of phosphotransfer-based dephosphorylation of DevR and /its single domain derivative, and (iii). the degree of dephosphorylation of phosphorylated species of DevS and Rv2027c and /their single domain derivatives, and a method of treatment, and a composition thereof.
US20090075917 Deuterium-enriched telithromycin The present application describes deuterium-enriched telithromycin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20100184776 Piperidine/piperazine derivatives The invention relates to a DGAT inhibitor of formula (I) including any stereochemically isomeric form thereof, wherein A represents CH or N; X represents O or NRx; the dotted line represents an optional bond in case A represents a carbon atom; Y represents a direct bond; —NRx—C(═O)—; —C(═O)—NRx—; —NRx—C(═O)—Z—; —NRx—C(═O)—Z—NRy—; —NRx—C(═O)—Z—NRy—C(═O)—; —NRx—C(═O)—Z—NRy—C(═O)—O—; —NRx—C(═O)—Z—O—; —NRx—C(═O)—Z—O—C(═O)—; —NRx—C(═O)—Z—C(═O)—; —NRx—C(═O)—Z—C(═O)—O—; —NRx—C(═O)—O—Z—C(═O)—; —NRx—C(═O)—O—Z—C(═O)—O—; —NRx—C(═O)—O—Z—O—C(═O)—; —NRx—C(═O)—Z—C(═O)—NRy—; —NRx—C(═O)—Z—NRy—C(═O)—NRy—; —C(═O)—Z—; —C(═O)—Z—O—; —C(═O)—NRx—Z—; —C(═O)—NRx—Z—O—; —C(═O)—NRx—Z—C(═O)—O—; —C(═O)—NRx—Z—O—C(═O)—; —C(═O)—NRx—O—Z—; —C(═O)—NRx—Z—NRy—; —C(═O)—NRx—Z—NRy—C(═O)—; —C(═O)—NRx—Z—NRy—C(═O)—O—; R1 represents optionally substituted C1-12alkyl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRx—C(═O)—Z—; —NRx—C(═O)—Z—NRy; —NRx—C(═O)—Z—C(═O)—NRy—; —C(═O)—Z—; —NRx—C(═O)—Z—NRy—C(═O)—NRy—; —C(═O)—NRx—Z—; —C(═O)—NRx—O—Z—; or —C(═O)—NRx—Z—NRy—; then R1 may also represent hydrogen; R2 and R3 each independently represent hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1-6alkyl; C1-6alkyloxyoptionally substituted with C1-4alkyloxy; C1-6alkylthio; polyhaloC1-6alkyloxy; C1-6alkyloxycarbonyl; cyano; aminocarbonyl; mono- or di(C1-4alkyl)aminocarbonyl; C1-6alkylcarbonyl; nitro; amino; mono- or di(C1-4alkyl)amino; —S(═O)p-C1-4alkyl; R4 represents hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1-6alkyl; optionally substituted C1-6alkyloxy; C1-6alkylthio; polyhalo-C1-6alkyloxy; C1-6alkyloxycarbonyl wherein C1-6alkyl may optionally be substituted; cyano; C1-6alkylcarbonyl; nitro; amino; mono- or di(C1-4alkyl)amino; C1-4alkylcarbonylamino; —S(═O)p-C1-4alkyl; R6R5N—C(═O)—; R6R5N—C1-6alkyl; C3-6cycloalkyl aryl; aryloxy; arylC1-4alkyl; aryl-C(═O)—C1-4alkyl; aryl-C(═O)—; Het; HetC1-4alkyl; Het-C(═O)—C1-4alkyl; Het-C(═O)—; Het-O—; R9 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
US20120322877 (bis)urea and (bis)thiorea compounds as eipgenic modulators of lysine-specific demethylase 1 and methods of treating disorders The invention provides for novel (bis)urea and (bis)thiourea compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer.
EP2708540A1 Pyrimido-diazepinone compound Provided are a compound represented by general formula (I), or the pharmaceutically acceptable salt thereof, (wherein Ra represents a hydrogen atom or the like, R1 and R2 may be the same or different, and each represents a hydrogen atom, optionally substituted lower alkyl or cycloalkyl, or R1 and R2 are combined together with the adjacent nitrogen atom thereto to form nitrogen-containing heterocyclic group, and Z represents a bicyclic heterocyclic group in which optionally substituted two six-membered rings are fused to each other, or the like) and the like.
WO2014160279A1 Stabilized cream formulations comprising sandalwood oil Provided herein are cream formulations comprising sandalwood oil, an antioxidant and a phosphate buffer. Also provided are methods of making and using the formulations. Further provided herein is a method of treating a skin disorder in a subject by administering to the subject a therapeutically effective amount of a cream formulation comprising sandalwood oil, an antioxidant and a phosphate buffer, wherein the subject has a skin disorder or is at risk of developing a skin disorder.
EP2139869A2 Axl kinase inhibitors useful for the treatment of cancer or hyperproliferative disorders Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.
WO2007143446A1 Spiro-condensed heterotricyclic compounds as hiv integrase inhibitors The invention encompasses series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
CA2585293A1 Lip enhancement compositions The present invention provides a cosmetic kit comprising: a first topical cosmetic composition comprising a physiologically tolerable vasodilator and at least one cosmetic carrier or excipient; a second topical cosmetic composition comprising a physiologically tolerable vasoconstrictor and at least one cosmetic carrier or excipient.
CN102379868A Antitumor medicament containing glycolysis inhibitor and preparation method and application of antitumor medicament The invention provides an antitumor medicament. The antitumor medicament is a glycolysis inhibitor, and the glycolysis inhibitor is 3-bromacetone acid ester. According to the antitumor medicament, the aim of killing tumor stem cells is fulfilled by efficiently blocking the energy metabolism of the tumor stem cells. The invention further provides application of the glycolysis inhibitor to the preparation of antitumor medicaments, a preparation method of the glycolysis inhibitor and application of the glycolysis inhibitor to tumor treatment.
CN101559065A Choerospondias extractive, preparation and application of phenol compound contained in choerospondias extractive The invention relates to a choerospondias extractive, a preparation method of phenol compounds contained in the choerospondias extractive, and the application of the extractive and phenol compounds in preparation of such functional foods as antihypoxia medicaments, antihypoxia health-care products, and the like.
WO2005003145A1 Shanzhuyu extract and uses thereof Provided are compositions and formulations containing an SZY extract or its active ingredients, loganin, morroniside, and cornuside. Also disclosed is a method of treating pain, autoimmune diseases, and inflammation using such compositions and formulations.
CN101904826A Arbidol HCl orally disintegrating tablet and preparation method thereof The invention relates to an arbidol HCl orally disintegrating tablet and a preparation method thereof. The arbidol HCl orally disintegrating tablet comprises the components based on parts by weight: 100.5-105.5 parts of arbidol HCl, 5.0-7.0% of hydroxy propyl cellulose, 20.0-30.0% of cane sugar powder, 50-100 parts of 2% povidone K-30 water solution, 40.5-50.5 parts of Eudragit E100, 15.5-16.5 parts of polyethylene glycol 6000, 3.5-5.5 parts of magnesium stearate, 500.0-700.0 parts of alcohol, 30.0-50.0 parts of microcrystalline cellulose, 7.0-9.0 parts of crosslinking povidone, 7.0-9.0 parts of crosslinking sodium carboxymethylcellulose, 7.0-9.0 parts of hydroxy propyl cellulose, 5.0-7.5 parts of aspartame, 0.2-0.7 part of menthol, 2.0-3.0 parts of magnesium stearate and 2.0-3.0 parts of food colorant. The invention comprises the steps of: pretreatment of raw materials and auxiliary materials, preparation of granules, coating of the granules, tabletting and packaging. The invention has simple technique control, rapid absorption, high bioavailability and convenient taking.
WO2008089260A2 Combined administration of benzonatate and guaifenesin Pharmaceutical compositions are provided containing a combination of benzonatate and guaifenesin, or pharmaceutically acceptable salts thereof. Methods of using compositions comprising benzonatate and guaifenesin, or pharmaceutically acceptable salts thereof, provide relief from cough, pulmonary congestion or both. The compositions and methods provide relief to opiate-sensitive individuals, in particular, as well as to infants and other pediatric patients.
CN1985994A Improved enteric medicine composition with mycophenolate The present invention relates to mycophenolic acid, and is especially a kind of improved medicine composition of mycophenolate with enteric coating. The medicine composition includes pharmaceutically acceptable mycophenolate with enteric coating, and the enteric coating includes poly(acetic vinyl phthalate) or acetic succinic hydroxypropyl methyl cellulose. The improved medicine composition of the present invention has excellent medicine releasing property.
CN1589835A Mulberry leaf extract and its use A mulberry leaf extract contains mulberroflavone, mulberropolyphenol, mulberropolyose, DNJ, GABA, etc and can be used to prevent and cure cardiovascular and cerebrovascular diseases, hyperlipemia, diabetes and obesity and delaying senility. It is prepared from mulberry leaves through drying in air, pulverizing, extracting and spray drying.
US7407938 1,4-Diphenyl-3-(3-hydroxy-3-phenylpropyl)-2-azetidinones, e.g., 2,3,4,5,6-Pentahydroxyhexylamide of 4-(4-{4-[3-[3-(4-fluorophenyl)-3-hydroxypropyl]-2-(4-methoxyphenyl)-4-oxoazetidin-1-y]lbenzylcarbamoyl}phenoxy)benzoic acid; antilipemic agents that have intestinal absorption of less than 10%, One embodiment of the invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification. Other embodiments of the invention relate to physiologically acceptable salts of compounds of formula I, to processes for their preparation and to medicaments comprising these compounds. The compounds of the invention are suitable for use, for example, as hypolipidemics.
US7060718 Novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
WO2007009697A1 Quaternary ammonium salts of substituted pyrazoline compounds, their preparation and use as medicaments The present invention relates to quaternary ammonium salts of substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
CN103536597A Application of Kadcoccitones A in preparing medicine for treating renal insufficiency The invention discloses application of Kadcoccitones A in preparing a medicine for preventing and/or treating renal insufficiency, and belongs to the technical field of new application of medicines. The application is disclosed for the first time. Since the framework type belongs to a brand new framework type and Kadcoccitones A high inhibitory activity on renal insufficiency, the Kadcoccitones A has outstanding substantive features; meanwhile, a remarkable progress is obviously made in preventing renal insufficiency.
WO2008148873A3 Hydroxyproline compositions and uses thereof The invention concerns novel use for Hydroxyproline in a pharmaceutical or dietary food or feed compositions for promoting growth e.g. of fish and/or for treating, ameliorating, or curing certain disorders including osteoporosis, psoriasis, enteritis and gingivitis.
US20090048276 Inhibitors of Fatty Acid Synthase (Fas) The instant invention provides for compounds which comprise substituted 3-aryl-4-hydroxyquinolin-2(1H)-ones that inhibit FAS activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting FAS activity by administering the compound to a patient in need of treatment of cancer.
US20080118578 topical chemotherapeutic mixture of Erythrosin B, Phloxine B, Rose Bengal, 4,5,6,7-Tetrabromoerythrosin or their salts in a hydrophilic vehicle containing sodium, potassium, calcium or magnesium chloride, phosphate, or nitrate for photodynamic therapy; osmolality greater than 100 mOsm/kg New photodynamic, topically-applicable medicaments and certain medical uses of such photodynamic medicaments for treatment of human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene. The halogenated xanthenes constitute a family of potent photosensitizers that become photoactivated upon illumination of the treatment site with visible wavelengths of light. In preferred embodiments, such medicaments are used for treatment of a variety of conditions affecting the skin and related organs; the mouth and digestive tract and related organs; the urinary and reproductive tracts and related organs; the respiratory tract and related organs; various other internal or external tissue surfaces, such as tissue surfaces exposed during surgery; and for treatment of a variety of conditions related to microbial or parasitic infection. In another preferred embodiment, such medicaments are produced in various formulations including liquid, semisolid or aerosol delivery vehicles.
CN102106805A Cymipristone solid preparation and preparation methods thereof The invention discloses preparation methods of a cymipristone solid preparation. A method 1 comprises the following steps: dissolving cymipristone in a solvent to obtain a drug-containing solution, then evenly mixing auxiliary materials with the drug-containing solution, and performing wet granulation, wherein, the solvent is an organic solvent or an aqueous solution containing more than 85% of an organic solvent by mass percent. A method 2 comprises the following steps: dissolving the cymipristone in an acid solution containing an acidulant to obtain a drug-containing acid solution, then evenly mixing the auxiliary materials with the drug-containing acid solution, and performing wet granulation. The invention further discloses the cymipristone solid preparation prepared by the methods. The preparation methods disclosed by the invention avoid the defects such as serious pollution, great loss and serious potential safety hazard caused by mechanical pulverization, and the methods are simple and feasible in operation and have a high safety factor, thus being applicable to industrial production. The cymipristone solid preparation prepared by the methods has the advantages of excellent leaching property, better stability and better content uniformity.
CN103230568A Benorilate vitamin B1 particle for children and preparation process thereof The invention belongs to the field of medical technology and discloses a benorilate vitamin B1 particle for children. The benorilate vitamin B1 particle for children is prepared from 0.3kg of benorilate, 3g of vitamin B1, 2.69g of sucrose, 3g of essence and 0.25g of tartrazine. The invention also discloses a preparation method of the benorilate vitamin B1 particle for children. According to the benorilate vitamin B1 particle for children, a good curative effect is brought to cold fever, the cold fever is not easy to relapse, less toxic and side effects are caused and the preparation process is simple and feasible.
WO2013148978A1 Methods and compositions for the treatment of necrotizing enterocolitis This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of necrotizing enterocolitis.
CN101747400B Lanostane type triterpenoid with anti-tumor activity, preparation method and application The invention discloses lanostane type triterpenoid with anti-tumor activity, a preparation method and the application of the lanostane type triterpenoid. The preparation method includes the following steps: ganoderma mycelium or an ethanol extract of sporocarp is prepared; the ganoderma mycelium or an ethanol extractum of the sporocarp is repeatedly extracted by petroleum ether after being dispersed by water, and is then extracted by ethyl acetate so as to obtain an ethyl acetate extract; the ethyl acetate extract is repeatedly separated by normal phase, opposite phase and gel column chromatography so as to obtain three parts; by utilizing the HPLC (high performance liquid chromatography), elution is carried out respectively by acetonitrile, methanol and water, and then the lanostane type triterpenoid is obtained through decompression and distillation drying after corresponding components are collected. Ganoderma sporocarp or fermented mycelium is separated to obtain 5 new lanostane derivants; in terms of the bioactivity, the newly-separated 5 lanostane derivants can effectively restrain proliferation of tumor cells and have excellent anti-tumor activity; therefore, the lanostanetype triterpenoid in the invention can be clinically applied as an anti-tumor agent.
US8741343 Method of administering amantadine prior to a sleep period Methods of nighttime administration of amantadine to reduce sleep disturbances in patient undergoing treatment with amantadine are described, as well as compositions of extended release amantadine that are suitable for nighttime administration.
US20070299044 Corticosteroid Topical Dispersion with Low Content of Surfactant The invention provides novel compositions of water-insoluble corticosteroid drug in combination with antimicrobial agents and very low concentrations of polymers and surfactants for topical, otic and ophthalmic treatment. The invention provides stable aqueous suspension where the ingredients remain in such a state so as to allow for immediate re-suspension, when desired, even after extended periods of settling. The invention provides also a method for treating inflammation with low systemic absorption and side-effects of the corticosteroid.
CN103230507A Genic health-care granule for keeping in-vivo alkalescence and preparation method of granule The invention discloses a genic health-care granule for keeping in-vivo alkalescence and a preparation method of the granule, and belongs to a nutrient product from plant extract. The preparation method of the genic health-care granule for keeping in-vivo alkalescence comprises the following steps of: soaking materials including flammulina velutipes, nepenthe, beetroot and the like for three hours by 0.5N sodium hydroxide; getting out the materials for mechanically crushing and juicing; carrying out sieving, ion exchanging, eluting, vacuum concentrating, CO2 supercritical extracting, re-concentrating and vacuum drying to the filtrate to obtain extract; and mixing the obtained extract with certain parts by weight of inositol, sucrose, taurine, citric acid and a nutrition metabolism acid-base equilibrium regulator to obtain the genic health-care granule. The genic health-care granule disclosed by the invention can be used for supplementing nutrition and energy which are likely deficient but necessary to the human body when the people drink water, is convenient to use and capable of solving an acidic problem of the human body, so that alkalescence in the human body is kept on the metabolism level. Moreover, the genic health-care granule suitable for keeping in-vivo alkalescence of different crowds including the middle aged and the elder, the female, the mental works, the athletes and the like.
CN103142566A Important-protein inhibitor in severe fever with thrombocytopenia syndrome The invention relates to virus replication inhibition using a small-molecular compound, and specifically discloses an application of a small-molecular compound suramin in preparing a medicine for treating a disease, wherein the disease is caused by viruses of bunyaviridae phlebovirus, and specifically by the viruses of severe fever with thrombocytopenia syndrome.
WO2012026609A1 Aqueous composition for ophthalmic administration An aqueous composition for ophthalmic administration which contains a β-blocker typified by, for example, timolol or carteolol and a sugar alcohol typified by mannitol or sorbitol optionally together with boric acid. The aforesaid composition can increase the corneal permeability of a drug. As a result, the drug dosage can be decreased, e.g., a lowering in the frequency of ophthalmic administration. Thus, it is expected that the risk of systemic side effects such as cardio toxicity or respiratory toxicity, which might be induced by the ophthalmic administration of the β-blocker, can be reduced thereby. It is also expected that a decrease in the frequency of ophthalmic administration would contribute to the improvement in QOL and prevent a decrease in the therapeutic effect caused by missed dose.
US20090088429 Isoquinoline Derivatives The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
US7126001 Antiproliferative agents; antitumor agents The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
US20110159070 Biomaterials and implants for enhanced cartilage formation, and methods for making and using them The invention provides products of manufacture, e.g., biomaterials and implants, for cartilage maintenance and/or formation in-vivo, in-vitro, and ex-vivo, using nanotechnology, e.g., using nanotube, nanowire, nanopillar and/or nanodepots configured on surface structures of the products of manufacture.
CN103609942A Pumpkin polysaccharide tablet and preparation method thereof The invention relates to functionalized food, and particularly relates to a pumpkin polysaccharide tablet with a blood glucose reduction function, and a preparation method thereof. The functionalized food comprises the following active ingredients in parts by weight: 120-400 parts of pumpkin polysaccharide powder, 90-300 parts of MCC (Microcrystalline Cellulose and Carboxymethylcellulose Sodium), 30-100 parts of sorbitol, 20-60 parts of PVP (polyvinyl pyrrolidone):PVP K30 (1:1), 5-15 parts of PEG6000, 5-15 parts of starch and 1-6 parts of magnesium stearate. The preparation method comprises the steps: respectively screening pumpkin polysaccharide powder and auxiliary materials through a sieve of 120-160 meshes, respectively weighing pumpkin polysaccharide powder, MCC, sorbitol, PVP:PVPK30(1:1), PEG (polyethylene glycol) 6000 and starch, evenly mixing, preparing wet granules and then fast drying, screening through a sieve of 14-24 meshes and straightening, adding the lubricant and evenly mixing, and tabletting to obtain the finished pumpkin polysaccharide tablet. The product is stable in active ingredients, unified in quality standards, good in bioavailability, convenient to take and carry.
CN102988998A Poloxamer-adriamycin conjugate with anti-tumor effect and preparation method thereof The invention discloses a poloxamer-adriamycin conjugate with an anti-tumor effect and a preparation method thereof. The poloxamer-adriamycin conjugate has micelle property, is a high-molecular polymer which contains terminal carboxyl group and is prepared by reaction between poloxamer and succinic anhydride, and the terminal carboxyl group in the polymer and primary amino radical in adriamycin are directly bound in an amido link way. Compared with an adriamycin raw material drug, the poloxamer-adriamycin conjugate has the following advantages: the anti-tumor activity of the covalent bonding adriamycin in the poloxamer-adriamycin conjugate is maintained, the drug resistance of tumor is reduced; the poloxamer-adriamycin conjugate has the property of self-assembly formed micelle, and the critical micelle concentration of the conjugate is lower than that of polyxamer; and the micelle of the poloxamer-adriamycin conjugate can be entrapped with other medicaments with the anti-tumor effect in a physical entrapping mode, so that the aim of combined treatment of anti-tumor medicaments can be achieved.
WO2012021287A2 Methods for the treatment and prevention of metabolic disorders Described herein are methods for detecting, characterizing, preventing, and treating metabolic diseases, including obesity and obesity-associated disorders such as diabetes.
CN101134043A Galenical for regulating and controlling blood sugar in physics method The botanic preparation for regulating blood sugar physically contains trigonella polysaccharide in 50-70 wt% and tea polysaccharide with the caffeine separated out in 30-50 wt%. The botanic preparation with high hydrophilicity can combine with water molecule inside gastrointestinal tract to form pectin-shaped cellulose to wrap decomposed carbohydrate mutually, so as to inhibit the absorption of carbohydrate in digestive tract effectively and slowly and to control blood sugar content in the source. The present invention realizes blood sugar regulating process during the food digesting, absorbing and metabolizing process, and the effective extract for regulating blood sugar does not enter to the blood circulation system and influence any body organs.
WO2009095394A1 Diazepanes as histamine h3 receptor antagonists The invention relates to compounds of formula (I) wherein R1 to R8 and X1, X2 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
US20080287497 Transdermal methods and systems for the delivery of anti-migraine compounds Iontophoretic patches for the delivery of anti-migraine compounds and methods of using the patches are described.
US20100122362 Cells expressing alpha-synuclein and uses therefor Disclosed are mammalian neuronal cells expressing alpha synuclein as well as methods of screening to identify compounds that decrease toxicity induced by alpha synuclein expression. Compounds identified by such screens can be used to treat or prevent synucleinopathies such as Parkinson's disease, familial Parkinson's disease, Lewy body disease, the Lewy body variant of Alzheimer's disease, dementia with Lewy bodies, multiple system atrophy, or the Parkinsonism-dementia complex of Guam.
WO2009070311A3 Crystal forms of o-desmethylvenlafaxine fumarate Provided are crystalline forms of O-desmethylvenlafaxine fumarate, methods for their preparation, and pharmaceutical compositions thereof.
WO2007000928A1 Remedy and/or preventive for chronic heart failure A preventive and/or a remedy for chronic heart failure which contains, as the active ingredient, a drug having an effect as a histamine H2 receptor blocker such as famotidine, cimetidine, ranitidine, roxatidine acetate, nizatidine or lafutidine. Namely, it is intended to provide a drug having an effect of reducing acute cardiac infarction size which is useful as preventive and a remedy for chronic heart failure.
US20090036432 Combinations of AT1-antagonists, amiloride or triamterine, and a diuretic The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising (i) an AT1-receptor antagonist or a pharmaceutically acceptable salt thereof, and (ii) the diuretic amiloride or triameterine or a pharmaceutically acceptable salt thereof, and (iii) a further diuretic or a pharmaceutically acceptable salt thereof.
CN101342178A Instant gel rubber of latanoprost for eyes The invention discloses immediate type ophthalmic gelatin of latanoprost and a preparation method thereof. 100 milliliters of the immediate type ophthalmic gelatin of latanoprost contains 0.1 to 2 grams of the latanoprost, 0.05 to 1 grams of preservative, 1.0 to 7.5 grams of permeation pressure conditioning agent and 30 to 150 grams of gelatin substrate. Remaining components are acid-base buffer regent and water for injection. The invention enriches the dosage forms of the latanoprost by optimizing auxiliary materials and improving technology so that lag time in eyes is greatly prolonged and a curative effect is improved without adverse stimulus reaction.
US20090029970 Pain remedy containing rock inhibitor Since a ROCK inhibitor exerts a potent analgesic effect by a single dose after the onset of a cartilage-related disease such as osteoarthritis, and can regenerate or suppress destruction of cartilage tissue and alleviate pain associated with cartilage diseases by multiple doses, administration of an therapeutically effective amount of the ROCK inhibitor to a patient with cartilage-related disease such as osteoarthritis or rheumatoid arthritis can treat the patient with cartilage-related disease and the ROCK inhibitor is thus useful.
WO2013024447A1 Compounds for use in cancer therapy Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds.
US20110269830 Statin nanoparticles The present invention relates to a complex made up of at least one molecule of statin or a derivative thereof, covalently bonded to at least one hydrocarbon radical including at least 18 carbon atoms and containing at least one 2-methyl-buta-2-ene unit, to nanoparticles of such a complex, and to a method for preparing same, said complex and/or said nanoparticles optionally being in the form of a lyophilisate. The present invention also relates to a pharmaceutical composition including at least one complex and/or nanoparticles such as previously defined. The invention finally relates to said complex and/or to said nanoparticles for the treatment and/or prevention of hyperlipemia and hypercholesterolemia.
US20050059694 Antiinflammatory and antiproliferative skin agents for Topical administration of treating skin psoriasis disease; lotions, gels, cream The compounds of formula I, have been found to have excellent topical activity. They are thus indicated for use in the topical treatment of inflammatory and hyperpoliferative skin diseases and of cutaneous manifestations of immunologically-induced illnesses, such as psoriasis.
US20120015903 PHARMACEUTICAL COMPOSITION FOR INHIBITING INCREASE OF IgA The present invention discloses a pharmaceutical composition for inhibiting increase of immunoglobulin A (IgA) comprising β-glucan and a pharmaceutical acceptable carrier. The β-glucan is extracted from Saccharomyces Cerevisiae, and the effective dose of the β-glucan is 300-450 mg/70 kg of body weights/per day, preferably, 350-400 mg/70 kg of body weights/day.
WO2014019485A1 New application of pogostone The present invention provides application of pogostone or a derivative thereof in preparing antibacterial drugs, health food, food, cosmetics, disinfectant, or everyday chemicals. The present invention also provides an antibacterial food, food, cosmetic, disinfectant, or everyday chemical. Pogostone has desirable inhibitory activity against pathogenic bacteria such as staphylococcus, or conditioned pathogens, can effectively treat bacterial infection diseases, and is also effective against methicillin-resistant bacteria, thus providing a new option for clinical medication.
EP1851739A2 Xanthurenic acid derivative pharmaceutical compositoins and methods related thereto The present invention relates to diuretic pharmaceutical compositions and methods and in particular to certain derivatives of the formula I: or a prodrug or pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.
CN103402514A Combinations of serotonin receptor agonists for treatment of movement disorders The present invention relates to the use of 5-HT1 agonists in pharmaceutical compositions, compounds and methods for treatment of movement disorders related to neurological dysfunctions. The invention is particularly relevant for treatment of patients suffering from tardive dyskinesia, Parkinson's disease and associated disorders thereof. Kits of parts comprising the 5-HT1 agonist compounds or pharmaceutical compositions according to the present invention, as well as methods of preparation are also provided by the present invention.
US20110118180 Method of treatment of diabetes type 2 comprising add-on therapy to metformin A method for the treatment of diabetes mellitus type 2 comprising administering (c) desPro36Exendin-4(1-39)-Lys6-NH2 or/and a pharmaceutically acceptable salt thereof, and (d) metformin or/and a pharmaceutically acceptable salt thereof, to a subject in need thereof.
US20050009822 7-(1-Acetylpentyl)-5-methyl-2-(4-methylbenzyl)imidazo[5,1-f][1,2,4]triazin-4(3H)-one; learning enhancement, concentration power, learning power, memory power; enzyme inhibitors of phosphodiesterase isoenzyme The invention relates to novel substituted imidazotriazinones, to a method for their production and to the use thereof for producing medicaments, in particular to improve perception, powers of concentration, learning capacity and/or memory retentiveness.
CN102908329A Divalproex sodium enteric-coated tablet and preparation method thereof The invention relates to a divalproex sodium enteric-coated tablet and a preparation method thereof. The divalproex sodium enteric-coated tablet is characterized in that divalproex sodium is easy to absorb moisture and uneasy to prepare an oral solid preparation; moreover, the moisture absorbing property of the oral solid preparation is reduced, the stability is enhanced, and better drug effect and less adverse reaction are obtained. According to the invention, a tablet core of the divalproex sodium enteric-coated tablet is prepared by an active component of the divalproex sodium and other medicinal excipients; a gastric soluble isolating layer and an outer enteric-coated film coating protective layer are coated outside the tablet core. Through the adoption of the divalproex sodium enteric-coated tablet provided by the invention, the moisture absorbing property of a preparation is obviously reduced as an ethanol solution of povidone is used as an adhesive, and the stability of the tablet is enhanced as a moisture-proof and lightproof coating agent with high adhesion is used for coating. The divalproex sodium enteric-coated tablet provided by the invention has the advantages of reasonable prescription, simple process, short production period, high efficiency, low cost, easiness in production, good preparation stability, good clinical effect, less adverse reaction and the like.
US20100021387 Methods for Inducing Reversible Stasis The present invention concerns compositions and methods involving incubating biological materials under hypoxic or anoxic conditions to induce stasis or suspended animation. Methods of screening for compounds that induce stasis or compounds that increase the ability to undergo stasis are included. Such methods have ramifications for preserving biological materials as well as reducing or preventing trauma to biological materials. Also contemplated are methods for screening compounds that are active or more active under hypoxic conditions than normoxic conditions. Such methods can be used to identify antitumor compounds that would operate under hypoxic conditions in which tumor cells survive.
CN102058575A Application of serine protease inhibitor to anti-embryo implantation and anti-tumor aspects The invention provides application of a serine protease inhibitor to anti-embryo implantation and anti-tumor aspects, and in particular discloses application of the serine protease inhibitor (an active derivative or pharmaceutically acceptable salt thereof) such as 4-(2-aminoethyl) phenylsulfonyl fluoride, gabexate mesilate and the like to the anti-embryo implantation and anti-tumor aspects. The invention also provides the application of the serine protease inhibitor to preparation of a composition or an appliance for suppressing embryo implantation or tumor cell growth.
US8263054 Method of enhancing hair growth Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R1 and R2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal. Bimatoprost is preferred for this treatment.
CN101066957A 4-hydroxy pyranone compound with substituting aryloxy methyl or arylthio methyl radical in 6-th place and its prepn and use The present invention is 4-hydroxy pyranone compound with substituting aryloxy methyl or arylthio methyl radical in 6-position and its preparation process and use. The present invention has the structure of the compound shown.
WO2008043825A3 Pharmaceutical anti-infective composition for inhalation. A composition for inhalation, comprising at least: a) an effective amount of an antimicrobial aminoglycoside derivative or a salt thereof, and b) an effective amount of a biofilm modifyer which is a macrolide derivative or a salt thereof.
CA2186953C Progesterone antagonists for the production of pharmaceutical agents for the treatment of dysfunctional uterine bleeding Competitive progesterone antagonists (antigestagens) are suitable for the production of pharmaceutical agents for the treatment of forms of dysfunctional uterine bleeding (metrorrhagias, menorrhagias, hypermenorrhea).
CN101422477A Compound apramycin sulfate injection The invention discloses a veterinary compound apramycin sulfate injection which can prevent pathogenic organisms from generating drug resistance. The invention belongs to medical products which contain organic effective components. Every 1000L of the compound apramycin sulfate injection is prepared by the materials as follows: 100 to 400kg of sodium salicylate and 20 to 100kg of maquindox are added into 300L of injection water in turn, stirred for 10 to 25min until the mixture is clear; then 30 to 120kg of apramycin sulfate, 1 to 20kg of atropine sulfate and 1 to 20kg of chlorphenamine maleate are added into another 300L of the injection water in turn, stirred and dissolved; then after the two obtained liquids are combined, the injection water is added to 1000L, fully stirred and maintained for 15 to 20min; and after the medicine liquid is clear, the veterinary compound apramycin sulfate injection is obtained. The invention adopts a compound preparation, is highly effective to the bacterial diarrhea of pig, treats both the symptom and root cause of diseases and eases the body stress response of an affected animal.
US20090291959 Caspase inhibitors based of pyridazinone scaffold The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.
EP1437137B1 Drugs comprising combination of antithrombotic agent with pyrazolone derivative It is intended to provide drugs for treating and/or preventing ischemic diseases which are safe and have little side effects. Namely, drugs comprising a combination of an antithrombotic agent and a pyrazolone derivative defined in the description or its pharmaceutically acceptable salt.
US7169927 Heterocyclic amides or prodrugs used in the treatment of diabetes, insulin resistance, metabolic disorders and obesity Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
US20080020990 Oligo Double-Stranded Rna Inhibiting the Expression of Bcl-2 and Pharmaceutical Composition Containing the Same The present invention relates to oligo double-stranded RNAs for use in knockdown of the expression of Bcl-2 protein known as a suppressor for apoptosis, and pharmaceutical compositions containing them. It is known that Bcl-2 protein is over-expressed in diseases such as cancer, and by this over-expression, the growth of cancer cells is continued and the drug resistance to anti-cancer agents is caused. The present invention provides highly active oligo double-stranded RNAs cleaving bcl-2 mRNA and further provides pharmaceutical compositions comprising a complex of the oligo double-stranded RNA and a suitable carrier for inhibiting the expression of Bcl-2 protein.
CN102942515A Ethane bridged indole compound, synthetic method and application thereof The invention discloses an ethane bridged indole compound, a synthetic method and an application thereof. The ethane bridged indole compound has a general structure formula shown as formula (I), wherein R' represents single-substituted or multi-substituted an aromatic ring, a heterocyclic ring or an indole ring. The ethane bridged indole compound has inhibited effects for cells of stomach cancer, lung cancer, breast cancer, intestinal cancer, liver cancer, multidrug resistant liver cancer, leukemia, cervical cancer, melanoma, ovarian cancer, neuroblastoma, nasopharynx cancer, lymjphoma and nephroblastoma. The ethane bridged indole compound having antineoplastic effects is reported for the first time herein. The synthetic method has the characteristics of mild reaction conditions, simple experimental steps, high yield, high product purity, economy and practicality, etc.
US20110300210 Controlled release nanoparticulate clozapine compositions Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.
CN101190192A Furosemide chewable tablets for dog or cat The invention discloses a furosemide chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the prior tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 10 to 30 percent of furosemide.
WO2010132864A1 Methods of treating hiv patients with anti-fibrotics The invention relates to methods of treating patients infected with human immunodeficiency virus (HIV) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.
US20120329747 Novel hydrazone derivatives having potent antitumor activity toward multi-drug resistant tumor cells A patentable new class of hydrazone derivative compounds is described, as are methods for synthesizing such compounds. The hydrazones of the invention can be used, for example, as potent anti-cancer agents, including to inhibit the growth of cancer cells that exhibit multidrug resistance.
US20110294819 Hepatitis C Virus Inhibitors The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
WO2014013090A3 Formulation comprising amorphous fingolimod The present invention relates to a solid composite of fingolimod base and a copolymer of methacrylic acid and divinylbenzene, a pharmaceutical formulation comprising said composite and the use of either the solid composite or pharmaceutical formulation as a medicament, particularly for the treatment of multiple sclerosis.
US8212057 Pyrroles having hypolipidemic hypocholesteremic activities, process for their preparation and pharmaceutical compositions containing them and their use in medicine The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine. The compounds lower triglyceride levels in blood and may be useful in the treatment of obesity, hyperlipidaemia, hypercholesteremia, syndrome X and diabetes.
CN101513400B Ampelopsin and basic amino acid solubilizing system and antitumor activity research The invention provides an ampelopsin composition and a method for preparing the same. The composition comprises: a) ampelopsin and b) a basic amino acid, wherein the weight ratio the component a) to the component b) is between 1:1 and 1:10. The composition can also comprise: c) a pH regulator and or d) a pharmaceutically acceptable carrier and/or a diluting agent. The invention also relates to a medicamnet box containing the ampelopsin composition and carboplatin. The ampelopsin composition can provide improved solubility, stability and a proper pH range and is suitable for clinic use.
US7655690 1-sulfonylindole derivatives, their preparation and their use as 5-HT6 ligands The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic), (I), (Ia, Ib, Ic), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or their salts, preferably their corresponding physiologically acceptable salts or corresponding solvates; to the processes for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them. The new compounds of the present invention can be used in the pharmaceutical industry as intermediates and for preparing medicaments.
CN102895256A Chitosan plural gel foaming agent suitable for female sperm shielding and killing dual-contraception effect and preparation method thereof The invention relates to a chitosan plural gel foaming agent suitable for a female sperm shielding and killing dual-contraception effect and a preparation method thereof, and belongs to the technical field of foaming agent production. The chitosan plural gel foaming agent suitable for the female sperm shielding and killing dual-contraception effect has a dual-contraception effect of vagina shielding and vagina sperm killing, and meanwhile has a fungal-infection-resistant effect. The foaming agent forms a medicament liquid by consisting of a matrix, a surface active agent, an auxiliary medicament, a cosolvent, an acidifier, a foaming agent, a foam stabilizing agent and a solvent, and the foaming agent and a propellent form a plural gel foaming agent according to the weight proportion of (100:10) to 20. The preparation method comprises the following steps: dissolving chitosan and carbomer into a citrate buffer solution with a certain amount; blending, heating to 80 DEG C to dissolve completely, adding the surface active agent so as to obtain a solution A; dissolving borneol, menthol crystal and stearic acid into glycerol, dissolving fully, and filtering so as to obtain a solution B; adding the solution B into the solution A, mixing fully, adding citric acid and SLS (sodium lauryl sulfate), supplying the buffer solution to the required weight, carrying out vacuum homogenizing for 2 hours, thereby obtaining the gel foaming preparation, and then adding the propellent.
CA2164842C Use of isovaleramide as a mild anxiolytic and mild sedative agent Isovaleramide has been found to exhibit mild anxiolytic (anxiety-reducing) activity at low to moderate dosage levels and mild sedative activity at somewhat higher dosage levels. In contrast to certain other materials thought to be anxiolytic or mildly sedative, isovaleramide is non-cytotoxic and does not paradoxically stimulate the central nervous system. Isovaleramide is therefore useful as a mild anxiolytic and mild sedative agent which can be made available to the general public.
WO2009150474A1 Dihydrotetrabenanzine for the treatment of anxiety The invention provides a 3,11b-cis-dihydrotetrabenazine of the formula (Ib): or a pharmaceutically acceptable salt thereof for use in the prophylaxis or treatment of anxiety.
CN101766623A Application of Morphine as antioxidant stress injury agent The invention relates to an application of Morphine as an antioxidant stress injury agent in medicaments, in particular to a new medical application of Morphine, belonging to the technical field of medicines. Through a thiazolyl blue (MTT) method, the Morphine is found to be capable of promoting the growth of adrenal gland chromaffin tumor cells (PC12 cells) of rats. The Morphine has the activity of promoting the proliferation of nerve cells and can inhibit nerve cell injuries caused by a Parkinson toxic substance MPP+(1-Methyl-4-Phenylpyridiniumion). Proved by a protein immunoblotting method, the Morphine can induce the expression level of thioredoxin in the PC12 cells, thus the Morphine for protecting the nerve cells from injuries of MPP+ toxicity is related to the induction of the expression of the thioredoxin.
CN102675141A N-(2-hydroxyethyl) erucic amide and preparation and application thereof The invention relates to N-(2-hydroxyethyl) erucic amide and preparation and application thereof. The invention discloses a structural formula of N-(2-hydroxyethyl) erucic amide, a chemical synthetic method for the N-(2-hydroxyethyl) erucic amide and application of the N-(2-hydroxyethyl) erucic amide in blood fat reduction. Experiments prove that the N-(2-hydroxyethyl) erucic amide has obvious effects of reducing blood fat, preventing or treating non-alcoholic fatty liver and protecting liver, and can be used for prevention and treatment of hyperlipidemia and non-alcoholic fatty liver caused by multiple reasons.
CN102370610A Anti-allergy medicine gel and preparation method thereof The invention relates to an anti-allergy medicine gel and a preparation method thereof. The gel adopts Desloratadine acid salts as main ingredients and is used for treating skin allergic inflammations. The anti-allergy medicine gel disclosed herein adopts Desloratadine acid salts as main active ingredients and uses beta-cyclodextrin, thus the dissolvability of Desloratadine in water is greatly improved, the skin permeability is improved, the content of free drug of local tissues of the partial skin that having the allergic inflammation of the organism is improved through transdermal absorption, the sensitization of histamine can be effectively prevented, the local anti-allergy anti-inflammatory curative effects are achieved, and adverse reactions are reduced.
US8586091 Pharmaceutical composition comprising N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-quinazolinamine The present invention relates to a pharmaceutical composition comprising N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine as active pharmaceutical ingredient and a process of preparing such composition.
US20090131338 Anesthesia arousal composition A method for facilitating postoperative awakening of patients from anesthesia does not depend on the experience of anesthesiologists. Also provided are an anesthesia arousal composition for use in this method and a preparation containing a bicarbonate ion that facilitates awakening from anesthesia. Specifically, the anesthesia arousal composition is provided in the form of infusion fluid. The method for controlling and facilitating awakening from anesthesia involves administering the anesthesia arousal composition. The present invention preferably provides an anesthesia arousal composition or an acidosis-correcting composition containing sodium bicarbonate as a major component that serves as a source of the bicarbonate ion, along with each or a combination of another electrolyte, glucose and an amino acid.
US20120015984 Granulate Formulation of Pirfenidone and Pharmaceutically Acceptable Excipients A capsule formulation of pirfenidone is provided that includes pharmaceutically acceptable excipients. In one embodiment, this capsule formulation is capable of sustaining desirable pharmacokinetic responses in a patient. Further provided are methods of treating fibrotic conditions and other cytokine-mediated disorders by administering pirfenidone capsules of such formulation to a patient in need.
US20050118205 Artificial sweetener, a sugar sweetener and a flavoring agent to mask a bitter antibiotic such as levofloxacin This invention is directed to a taste masked liquid pharmaceutical composition comprising a pharmaceutically active agent and a taste masking composition. In particular, the taste masking composition comprises a taste masking effective amount of an artificial sweetener.
WO2011160920A1 Dry powder formulation comprising an antimuscarinic drug The invention relates to a dry powder formulation suitable for the inhalatory administration by means of a dry powder inhaler, comprising an antimuscarinic drug as active ingredient. The invention also relates to the process for the preparation of the formulation and to its use in the prevention and/or treatment of a wide range of conditions including respiratory disorders.
US20110020425 Materials and methods for wound treament The subject invention pertains to methods and compositions for wound treatment. The methods and compositions provide for promoting and accelerating wound healing; provide for inhibition of microbial infection; provide for a protective scab-like covering on a wound; and/or for arresting the flow of blood or body fluids from an open wound. The methods and compositions can be used to increase granulation and epithelialization in a wound. In one embodiment, a substantially anhydrous compound of a salt ferrate and a cation exchange material is provided. Compositions of the invention can also include silver compounds. In use, compositions of the invention are preferably applied as a dry dressing to an exuding chronic wound site. If the chronic wound site is dry, the wound site may be wetted with a suitable liquid or aqueous media prior to applying the dressing in dry form.
US20110274725 Decomposable biocompatible hydrogels and system and method for using same Biocompatible, triggerable degradation, polymerizable hydrogels, uses and delivery devices are disclosed. These hydrogels are at least substantially water soluble macromers, having a variety of uses especially for ocular therapy. The macromers include at least one water soluble region, at least one region which is degradable via a triggering event, usually by hydrolysis, and at least two free radical-polymerizable regions. The regions can, in some embodiments, be both water soluble and trigger able degradable. The macromers are polymerized by exposure of the polymerizable regions to free radicals generated by photosensitive chemicals and dyes. An advantage of these polymer hydrogels is that they can be polymerized rapidly in an aqueous surrounding. Precisely conforming, semi-permeable, biodegradable films or membranes can thus be formed on tissue in situ to serve as biodegradable barriers, as carriers for living cells or other biologically active materials, and as surgical adhesives for the eye.
WO2013154570A1 Synthetic mechanical hemostatic composition, method of making and use thereof A biocompatible, polymeric composition is disclosed. The composition comprises a base polymer comprising (i) a prepolymer comprising para-dioxanone (PDO) and trimethylene carbonate (TMC); and (ii) an end-graft polymer chain comprising a polylactone. Also disclosed are a method for treating bleeding from bone or bony structures using the composition, a method for filling a void or correct a defect in a bone using the composition, and a method for producing the biocompatible, polymeric composition of the present application.
CN102993175A Dabigatran derivatives, and preparation method and application thereof The invention belongs to the technical field of medicine, and specifically relates to a preparation method of a benzimidazole derivative represented by a general formula I. R1 and R2 are respectively as defined in the specifications. The invention relates to Dabigatran derivatives represented by a general formula I, nontoxic and pharmaceutically acceptable salts thereof, medicine compositions containing the compounds as active components, and applications of the compounds and medicine compositions as thrombin inhibitors. The general formula I is represented below.
CN102697793A Medicament for inhibiting oral bacterial plaque and preparation method thereof The invention relates to the field of oral medical treatment, in particular to a medicament for inhibiting oral bacterial plaque and a preparation method thereof. The medicament for inhibiting the oral bacterial plaque comprises gallnut tannic acid serving as a raw material and aids. The medicament comprises the following raw materials in part by weight: 4 to 8 parts of gallnut tannic acid, 200 to 300 parts of mannitol, 200 to 250 parts of sucrose particles, 10 to 20 parts of citric acid, 5 to 15 parts of blueberry essence, and 2 to 5 parts of magnesium stearate. The raw materials containing the gallnut tannic acid are prepared into tablets. By adopting the technical scheme, the medicament has the advantages that the chewable gallnut tablets can effectively control bacteria and bacterial plaque by chewing so as to inhibit dental caries; oral health can be effectively kept in special environments of water shortage; and particularly, the incidence of rampant caries, irritable oral ulcer, pericoronitis, plateau hypoxic gingivitis and periodontitis in a stress state is reduced.
CN101785761A Compound hemostasis medicine and preparation method thereof The invention provides a compound hemostasis medicine, namely a compound adrenal color hydrazone enteric capsule formulation or granular formulation, mainly containing adrenal color hydrazone, vitamin K1, vitamin C and pharmaceutic adjuvants. By using the invention, the defect lacking of blood coagulation function for the existing adrenal color hydrazone hemostasis medicine is solved to reduce blood capillary permeability and enable an injured blood capillary end to retract to realize hemostasis effect; vitamin K1 is used for affecting some blood coagulation factors and promoting or restoring blood coagulation process to speed up hemostasis; vitamin C containing synthetical collagen and histocyte is used for repairing injured blood capillary wall in time, stimulating blood coagulation function and promoting wound to heal; and the enteric formulation enables the medicine to release in intestines to effectively reduce stomach stimulation and adverse reaction of salicylic acid reaction caused by adrenal color hydrazone release in stomach. The invention also provides a method for preparing the compound adrenal color hydrazone enteric capsule formulation or granular formulation.
WO2014155301A1 Substituted bicyclic compounds as inhibitors of ezh2 The present invention provides compounds of formula 1, isotopic forms, stereoisomers or tautomers thereof, or pharmaceutically acceptable salts, solvates, N-oxides, S-oxides and polymorphs thereof, and processes for their preparation. The invention further relates to pharmaceutical compositions containing said compounds and their use in the treatment of diseases or disorders mediated by EZH2 (enhancer of zeste homolog 2), particularly cancer.
US6943182 Cyclopentabenzofuran derivatives and their use The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-κB-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.
CN103550237A Composition of active ingredients of rubia cordifolia as well as application of composition in medicines The invention relates to an active extract composition of rubia cordifolia with exact pharmacologic action. The composition is characterized by comprising 1, 3, 6-trihydroxyl-methyl anthraquinone-3-O-alpha-rhamnose (1->2)-beta-glucoside and mollugin, and the total content of the two active ingredients is greater than 90%. The weight ratio of the 1, 3, 6-trihydroxyl-methyl anthraquinone-3-O-alpha-rhamnose (1-2)-beta-glucoside to the mollugin in the composition is 1:(0.5-5). The invention further relates to an application of the active extract composition of rubia cordifolia in preparing medicines for treating leucopenia.
CN103655584A Medicine dehydration mixture for treating encephaledema The invention relates to a medicine dehydration mixture for treating encephaledema, which can effectively achieve rapid dehydration and no toxic or side effects for treating the encephaledema. The medicine dehydration mixture adopts the technical scheme that the medicine dehydration mixture is prepared by adding and uniformly dissolving 4-6mg dexamethasone and 10-15mg furosemidum into 100-125ml mannitol at a volume concentration of 20%. The medicine dehydration mixture is rich in raw material, convenient to use, easy to produce, low in cost, safe to use, free from toxic or side effects, and good in curative effect and treats the encephaledema rapidly and effectively.
EP1685100B1 Novel 1, 3-disubstituted azetidine derivatives for use as 5ht2a receptor ligands Compounds of formula (I): are antagonists of the human 5-HT2A receptor, and hence useful in treatment or prevention of a variety of neurological conditions.
CN102766145A Fluorinated aza imidazolone derivative, synthesis method and application thereof The invention relates to a fluorinated aza imidazolone derivative, a synthesis method and application thereof. The derivative has the following structural formula: a, wherein R is -H, -Cl or -OCH3; n = 1 or 2; b, wherein R1, R2, and R3 is -H or a fluorinated methyl. According to the invention, the impact of different structures on the pharmaceutical activity and neurotoxicity of a compound is studied so as to expect to find a lead drug with good activity and low toxicity; the pharmacological evaluation of fluorinated imidazole bicyclic compounds is conducted, the anticonvulsant activity is respectively determined by a mouse maximal electroconvulsive test (MES) and a rat anti-pentylenetetrazol experiment (PTZ), and the neurotoxicity is determined by a rotary method. The results show that the compound has the characteristics of excellent activity and low toxicity, and is an excellent antiepileptic drug precursor.
WO2014097147A1 Tricyclic compounds as cftr inhibitors The present invention provides a CFTR inhibitor of formula (I) or a pharmaceutically acceptable salt thereof; and its therapeutic uses, e.g. in the treatment of diarrhea. The present invention further provides a combination of pharmacological active agents and a pharmaceutical composition.
US20110071120 Solid state forms of tapentadol salts Provided herein are novel solid state forms of tapentadol salts, process for their preparation, pharmaceutical compositions, and method of treating thereof. The tapentadol salts include an L-(−)-camphorsulfonate salt, a dibenzoyl-(L)-tartrate salt, a dibenzoyl-(D)-tartrate salt, a malate salt, a maleate salt, or a salicylate salt.
WO2012162108A2 Boron-containing compositions and methods therefor Contemplated boro-carbohydrate compounds are demonstrated to modulate the blood concentrations of various polypeptides associated with metabolic syndrome by administration of a tetrahedral, and under-carboxylated osteocalcin, adiponectin, and YKL-40. Use of such compounds in oral administration is especially preferred and may be effective to address one or more components of metabolic syndrome.
US7183112 Administering locally to the area of inflammation to an animal an anti-inflammatory effective amount of an anti-malaria compound which is aminoquinoline or derivative A diversity of inflammatory diseases can be treated via local delivery to the patient of a composition containing a therapeutically effective amount of an anti-malarial agent. In a preferred embodiment of the method of the invention, a pulmonary inflammatory condition, such as asthma, is treated by inhalation of an aerosolized anti-malarial agent, such as hydroxychloroquine.
WO2014006569A3 Saxagliptin salts The present invention provides saxagliptin bisulphate, saxagliptin acetate, saxagliptin oxalate, saxagliptin bicarbonate, and saxagliptin carbonate, their polymorphic forms, processes for their preparation, and pharmaceutical compositions thereof.
WO2007116866A1 Hetero compound It is intended to provide a useful compound as an active ingredient of a preventive and/or therapeutic agent for rejection in the transplantation of an organ, bone marrow, or tissue, an autoimmune disease or the like which has an excellent S1P1 agonist effect. Because the compound of the invention has an S1P1 agonist effect, it is useful as an active ingredient of a therapeutic agent or a preventive agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or tissue or graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, or ischemia-reperfusion injury or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer or leukemia.
CA2565698A1 Benzimidazoles, method for producing them and the use thereof as drugs The invention relates to the novel substituted benzimidazoles of general formula (I), wherein R1 to R6 are defined as in claim 1, to the tautomers, enantiomers, diastereomers, mixtures and salts thereof, especially the physiologically acceptable salts thereof with inorganic or organic acids or bases. The novel substances have valuable properties.
CN1810816A Tenoforv monoester compounds with HIV-1/HBV virus copying inhibiting activity The present invention relates to one group of Tenofovir monoester compounds and their alkali/acid composites, synthesis process and antiviral application. Extracorporeal experiment shows that the compounds of the present invention have HIV-1 virus copy and HBV virus copy inhibiting activity. The present invention lays foundation for the research and development of the compounds in antiviral application.
CN103446156A Application of caffeine in preparing anticoagulation medicine The invention discloses an application of caffeine in anticoagulation, which belongs to the field of application of natural compounds in medicines. The caffeine (1,3,7- trimethyl xanthine) is used as a chemical medicine in anticoagulation and antithrombus. After the Balb/c mouse is subjected to the intragastric administration of the caffeine at the dosage of 80mg/kg for half an hour, both the tail bleeding time and the in-vitro coagulation time of the mouse are obviously longer than those of the mouse in a control group. The caffeine is relatively safe and free from side effect, and can be used for preventing and treating the thrombogenesis.
EP2266665A1 Method for the improvement of islet signaling in diabetes mellitus and for its prevention The present invention discloses a method for therapeutically treating mammals, including but not limited to humans, to increase the relative insulin producing performance of endogenous pancreatic β-cells and to cause differentiation of pancreatic epithelial cells into insulin producing β-cells. Oral administration of a DP IV inhibitor causes the active form of GLP-1 to be preserved longer under physiological conditions. The extended presence of GLP-1, in particular in the pancreatic tissue facilitates differentiation and regeneration of the β-cells already present that are in need of repair. These repaired insulin producing cells can contribute to the correction and maintenance of normal physiological glycemic levels.
WO2014124013A1 Amino diol derivatives as sphingosine 1-phosphate (s1p) receptor modulators The present invention relates to amino diol derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
WO2014099503A1 Triazolone compounds and uses thereof The invention disclosed herein is directed to compounds of Formula I [Formula should be inserted here] and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a therapeutically effective amount of a selective PPARa antagonist. The compounds and pharmaceutical compositions of the invention are also useful in the treatment of viral infections, such as HCV infections and HIV infections.
WO2006137789A8 Quinoline 3 -sulfonate esters as NK3 receptor modulators Compounds of Formula I wherein R1, A, R2, R3, R4, R5 n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
EP1656131B1 Use of betaine for treating intermittent claudication The invention describes the use of betaine for treating and preventing arteritis. The invention also describes an orally administered composition for treating arteritis and, in particular, intermittent claudication, said composition containing, as an active ingredient, an active therapeutic quantity of betaine glycine by single dose. The invention particularly describes a medicament provided for treating a patient suffering from an intermittent claudication caused by peripheral circulatory disorders such as arteriosclerosis obliterans or by thromboangiitis obliterans.
WO2006049880A1 Tetrahydro pyridinyl pyrazole cannabinoid modulators This invention is directed to a tetrahydro-pyridinyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
WO2009059989A1 Aqueous emulsions comprising a hydrophobic active ingredient The invention relates to aqueous emulsions comprising a hydrophobic active ingredient, to methods for the production thereof, pharmaceutical compositions, such as therapeutic agents, diagnostic agents, and/or prophylactic agents, in particular anesthetic agents, which comprise the aqueous emulsions, to the use of the aqueous emulsions to produce medications, and to methods for the therapeutic and/or prophylactic treatment of the human or animal body and/or for diagnosis by administration of the aqueous emulsion.
WO2005032515A1 New use, pharmaceutical preparations as well as a process for their production The invention concerns the use of mercaptoethane sulfonate-sodium (Mesna) to increase the solubility of the Ifosfamide in storage-stable, concentrated and/or highly-concentrated (supersaturated) aqueous pharmaceutical Ifosfamide preparations for parenteral administration as well as a process for their production.
US20080139532 Tetrahydrobenzazepine Derivatives as Modulators of Dopamine D3 Receptors (Antipsychotic Agents) The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. as agents to treat various aspects drug dependency or as antipsychotic agents.
CN101732318A Antiviral medical composition containing penciclovir and preparation method thereof The invention provides antiviral medical composition containing penciclovir and preparation method thereof. The composition comprises penciclovir, water, sodium hydroxide and an optional isotonic agent. Compared with the traditional penciclovir preparation, the invention has obvious advantages that the sodium hydroxide can be salified with the penciclovir, thus the solubilizing effect is obvious, and other cosolvents or organic solvents do not need to be added, thereby avoiding clinical side effects, simplifying the preparation process, reducing the production cost and being beneficial to environmental protection. The pH value of the composition is 10.5-11.5, and the stability of a product is the best, thus the composition is suitable for industrial production, transport and storage. When the composition is used as an injection for clinical use, the pH value of the composition is controlled to be 7.0-9.0, and various quality indexes are stable; and when the composition is applied to the human body, the composition cannot generate serious phlebitis and is easy to accept by patients. A proper quantity of active carbon is adopted in the preparation method; and besides guaranteeing to remove bacteria and pyroxene, the active carbon has no influence on the pH value of the product, and the loss of active constituents is reduced.
CN101006072A Novel sulfamate and sulfamide derivatives useful for the treatment of epilepsy and related disorders The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical composlons containing them and their use in the treatment of epilepsy and related disorders.
US7414063 e.g. 2-(2-bromo-4-fluoro-phenoxy)-ethyl]-[2-(isoquinoline-5-sulfonylamino)-ethyl]-carbamic acid tert-butyl ester; serine/threonine kinase inhibitor; anticarcinogenic agent; solid tumor, leukemia The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
EP1089738B1 Antimicrobial compositions comprising taurolidine, citric acid and sodium citrate The present invention relates to a method of inhibiting or preventing infection and blood coagulation in or near a medical prosthetic device after said device has been inserted in a patient comprising administering to the device a pharmaceutically affective amount of a composition comprising: (A) at least one taurinamide derivative, and (B) at least one compound selected from the group consisting of biologically acceptable acids and biologically acceptable salts thereof, whereby there are no systemic anticlotting and no systemic biocidal effects.
CA2769652A1 Macrocyclic serine protease inhibitors useful against viral infections, particularly hcv Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula (Ia) or (Ib), pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
WO2013169194A1 Treatment of postpartum haemorrhage with chemically modified heparin or heparan sulphate and a uterotonic agent The present invention refers to the use of certain sulfated glycosaminoglycans for treatment or prevention of postpartum haemorrhage. The sulfated glycosaminoglycans have a reduced anticoagulant activity and are administered in combination with at least one uterotonic agent capable of promoting myometrial contractions of the uterus and thereby compress the vessels and cease the bleeding.
WO2010048880A1 The nitropyridinyl ethyleneimine compound, the pharmaceutical composition containing it, the preparation method and use thereof The nitropyridinyl ethyleneimine compound as the general formula I, its preparation method, its use for the manufacture of a prodrug, and its use for the manufacture of a medicament of treating tumor.
WO2014014901A1 Octahydro-cyclopentapyrrolyl antagonists of ccr2 The present invention comprises compounds of Formula (I). Formula (I) wherein: R1, R2, R3, R4, R5, Z1 and Z2 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
US6958345 syn-N1-(2-hydroxymethylcyclopropylidenemethyl)-cytosine for example; treating HIV, herpes viruses, Epstein-Barr virus (EBV), hepatitis B virus Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.
WO2012121140A1 Growth hormone secretion promoter The purpose of the present invention is to provide a growth hormone secretion promoter which has an excellent growth hormone secretion promoting effect and can be administered orally. This growth hormone secretion promoter contains at least one component selected from the group consisting of S-adenosylmethionine and/or a salt thereof, a Siberian larch extract, an olive extract and a stilbene compound as an active ingredient. S-Adenosylmethionine and/or a salt thereof may be contained in a chemically synthesized form thereof which is not modified in any way, or cells or a culture each containing S-adenosylmethionine and/or the salt thereof may be contained. The stilbene compound may be an extract from a plant belonging to the family Vitaceae or Gnetaceae. The olive extract may be an extract separated from an olive fruit.
WO2013171167A1 A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome The present invention relates to methods for treating and/or preventing podocytes related disorders and/or nephrotic syndrome comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for treating and/or preventing a metabolic disease in a patient with or at risk of podocytes related disorders and/or nephrotic syndrome.
US20120295914 Combination of adrenergic receptor agonist alpha-1 or alpha-2, preferably brimonidine with fillers, preferably hyaluronic acid A combination of a quantity of adrenergic receptor agonist α-1 or α-2, and preferably product known as brimonidine, with fillers, and preferably with hyaluronic acid, for decreasing skin or cutaneous reactions is described.
WO2007093184B1 Treatment of mmp-mediated dermatological diseases with pemirolast The invention relates to compounds for the treatment of dermatological diseases where inflammation, matrix metalloproteinases (MMPs) and peroxisome proliferator- activated receptors (PPARs) play a role in mediating the disease, such as the 5 treatment of acne with Pemirolast or a closely related compound thereof.
WO2010027567A3 Tricyclic spirocycle derivatives and methods of use thereof The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disoder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
CN102091148A Coating method for miraculous pill of ledebouriella The invention belongs to the technical field of medicinal herb processing, and in particular relates to a coating method for miraculous pill of ledebouriella. The invention aims to solve the problems that the coating of the traditional miraculous pill of ledebouriella is easy to fall off, a large amount of acacia mucilage, peach gum and gelatin are used in the coating method, thus resulting in increase of the production costs and pollution of the environment, and serious waste of glutinous rice is caused. The invention has the technical scheme that the coating method for the miraculous pill of ledebouriella comprises the following steps: (1) crushing talcum powder into fine powder; (2) crushing glutinous rice into glutinous rice powder, putting the glutinous rice powder into a container, adding cold water to form paste, then adding hot water and mixing to form transparent paste for preparing a bonding agent; (3) putting the miraculous pills of ledebouriella, the fine powder and the bonding agent in a certain proportion into a coating machine for coating to obtain coated miraculous pills of ledebouriella; and (4) baking the coated miraculous pills of ledebouriella in an oven to obtain the finished product of the miraculous pill of ledebouriella. The invention has the advantages of low production cost, good coating effect and the like.
CN101524422A Health products with hypolipemic function, preparation method and usage thereof The invention relates to health products with hypolipemic function and also relates to a preparation method for the health products and the usage thereof. The health products comprise active constituents of hongqu powder, hawthorn extract, ginkgo biloba leaf extract, obtuseleaf senna seed extract and radix salviae miltiorrhizae extract. The active constituents have very obvious synergistic effect, thus playing a positive role in hypolipemic in many aspects such as reducing endogenous lipid synthesis, promoting the transfer and excretion of lipid, regulating lipid metabolism and the like, having obvious hypolipemic effect; safety toxicity test proves that the active constituents are safe, innoxious and harmless.
US20080233059 Heating and reacting polyglycerol with ricinoleic acid or another hydroxyl fatty acid to polymerize; maintaining temperature until reaction mixture reaches a desired acid value; esterification, condensation polymerization, catalysis with acid or basic catalyst; cosmetics, sunscreen agents, dairy products A process for manufacturing polymers of glycerin and hydroxyl fatty acids, for example, polyglycerol polyricinoleates, which mix a polyglycerol with a hydroxyl fatty acid directly to form a reaction mixture, and then heat the reaction mixture to a temperature sufficient to cause it to polymerize through an esterification mechanism until the reaction mixture reaches a desired acid value.
CN101948716A Anhydrous hand washing agent The invention discloses an anhydrous hand washing agent, which consists of alkyl benzene sulfonic acid, white mineral oil, span-20, deodorized kerosene, morpholine, lecithin, sodium hydroxide, resin finishing agent HMV, aqueous ammonia, solvent oil, soap flake, essence and deionized water in percentage by weight. The anhydrous hand washing agent is prepared by the following steps of: mixing the alkyl benzene sulfonic acid, white mineral oil, span-20, deodorized kerosene, morpholine, lecithin, sodium hydroxide, resin finishing agent HMV and aqueous ammonia together, putting the mixture into a container, heating and dissolving the mixture with stirring, adding 70 DEG C water into the mixture with stirring, adding the solvent oil and the soap flake into the mixture with stirring when the mixture forms dilute emulsion, then slowly stirring the mixture and cooling the mixture to 50 DEG C, adding the essence into the mixture, and continuously cooling the mixture to 35 DEG C with stirring to obtain a finished product of the anhydrous hand washing agent.
CN103463014A Compound alpha-ketoacid tablet and preparation method thereof The invention relates to a compound alpha-ketoacid tablet free from talcum powder and a preparation method of the tablet. The tablet prepared by using the preparation method is good in compressibility, beautiful in appearance, high in disintegration speed, high in dissolution rate and high in long storage stability. According to the preparation method provided by the invention, a dry granulation method is used, all the ingredients are prevented from contacting water or other wetting agent, and therefore, the tablet can be stably stored for long time, and the content of effective ingredient is ensured. The content of the polyethylene glycol in the prescription is optimized, the talcum powder or the analogue with composition similar with that of the talcum powder are not contained in the prescription, no disintegrating agent needs to be added, the problems of clustering phenomenon and quite large viscidity in a wet granulation process in the traditional production are solved, the medication safety is ensured, and the product can be stably produced with quality and high safety.
CN101230015B Substituted cinnamic acid derivatives containing amine substituent group and tumor cytotoxicity thereof The invention relates to a substituted cinnamic acid derivatives comprising amides substituent with a structure shown as Formula (I) and cytotoxic activity as well as medicine salts or solvates of the derivatives. The invention also relates to the preparation method and medicine purpose of the compounds with a Formula (I) The compounds of invention are provided with the activity of inhibiting growth of human oral squamous carcinoma cells, namely KB cell. The derivatives can be expected to be used as an antitumor drug.
US20080063601 treatment of urogenital disorders comprising administering calcium channel blockers, such as triptolide, prodrugs and/or derivatives Described herein are therapeutic strategies (methods and compositions) useful for treating conditions in which cilia are affected and which manifest with cysts and/or fibrosis, such as conditions in which the kidney, pancreas, liver and/or spleen are affected and contain cysts. Particular embodiments described herein are therapeutic strategies in which PC-2 agonists, particularly agonists (calcium channel agonists) that target PC-2 directly and/or selectively, are administered to individuals with mutations in PKD1, in order to alter the course of polycystic kidney disease, particularly ADPKD. In specific embodiments, the invention relates to use of PC-2 agonists triptolide and triptolide derivatives to regulate calcium release. In other aspects, the invention relates to use of PC-2 agonists to treat or aid in the treatment of any condition in which a calcium channel, such as the gene product of PKD1 and/or PKD2, is mutated; calcium signaling is abnormal; or both.
WO2006094627A3 Use of hydroxy tetrahydro-naphtalene derivates for the treatment of respiratory diseases This invention relates to new uses of hydroxy-tetrahydro-naphthalenylurea derivatives which are described in WO 03/095420 as an active ingredient of pharmaceutical preparations for the treatment of diseases associated with VR1 activity. The new uses of the present invention are the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of respiratory diseases or disorders such as the common cold, cough, sneeze, bronchitis including acute and chronic bronchitis, bronchiolitis, rhinitis, allergic rhinitis, vasomotor rhinitis, mucositis, sinusitis, allergy, disorders associated with exogenous irritants such as tobacco smoke, smog, high levels of atmospheric SO2 and noxious gases in the workplace, and airways hyperreactivity, milk product intolerance, Loffler's pneumonia, emphysema, cystic fibrosis, bronchiectasis, pulmonary fibrosis, pneumoconiosis, collagen vascular disease, granulomatous disease, laryngitis, pharyngitis, pneumonia, pleuritis, persistent asthma and chronic asthmatic bronchitis.
EP2328891A1 New benzofurans suitable as precursors to compounds that are useful for imaging amyloid deposits The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.
US20120315281 Treatment of renal injury Methods for the treatment of renal injury include the use of arginase inhibitors in the treatment and prevention of diabetic nephropathy, albuminuria and azotemia amongst others, and methods for identifying agents for the treatment of renal injury.
CN103006584A Preparation method of injection pemetrexed disodium The invention relates to a preparation method of injection pemetrexed disodium. The preparation method comprises the following steps of: 1) weighing lactose, adding half injection water, heating to 40 DEG C to dissolve the lactose to obtain an auxiliary liquid at a temperature of 40 DEG C; 2) stirring for 30 minutes with 20g of activated carbon, and filtering the activated carbon; 3) weighing a pemetrexed disodium raw material, adding to the decarbonized auxiliary liquid, and quickly stirring until the pemetrexed disodium raw material is completely dissolved; 4) adding injection water to 19L, regulating the pH value to be between 6.8 and 7.4 with sodium hydroxide or hydrochloric acid, and adding injection water to 20L; and 5) filling, and lyophilizing by adopting a vacuum lyophilization technology, wherein the pre-freezing temperature is minus 40 DEG C for 2 hours, the lyophilizing time is 18 hours, the analytical drying time is 3 hours, and the method totally costs 23 hours.
US20060014679 Drug screening; diabetes, obesity, hyperlipemia, arteriosclerosis, hypertension, cardiovascular disorders A compound or its salt inhibiting the activity of a protein having an amino acid sequence which is the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, an extracellular domain of the protein above, an antibody, an antisense polynucleotide, etc. are usable as insulin-sensitizing agents and preventives and/or remedies for diabetes, obesity, hyperlipemia, arteriosclerosis, hypertension, heart disease, and so on.
CN101138545A Clathrate compound containing ginsenoside Rg2 and method of preparing the same The present invention discloses an inclusion complex containing the panaxsaponin Rg2 and the preparation method. The inclusion complex of the invention consists of the panaxsaponin Rg2 and the hydroxypropyl-Beta-cyclodextrin. The preparation method of the present invention is as following. The hydroxypropyl-Beta-cyclodextrin water solution is prepared; the hydroxypropyl-Beta-cyclodextrin solution is kept in the water bath; the extraction powder of the panaxsaponin Rg2 or the extraction of the liquid-typed Rg2 dissoluted by the solvent is added before mixing and complex; therefore the liquid inclusion complex is obtained and the inclusion complex after drying. The inclusion complex of the present invention has functions of increasing the heart perfusion and the blood flow, expanding the diameter of the vein and the artery, improving the microcirculation disturbance, improving the myocardial ischemia and anti-thrombosis effect. The present invention can significantly reduce the acute toxicity of the panaxsaponin Rg2.
WO2014091297A1 Spirocyclic morphinans and their use The application is directed to compounds of Formula (I'-Α), and especially to compounds of Formula (I-A) and pharmaceutically acceptable salts and solvates thereof, wherein R1a-R5a, Y, Za are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I'-Α), and especially compounds of Formula (I-A), to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
EP1450781B1 Formulation of amino acids and riboflavin useful to reduce toxic effects of cytotoxic chemotherapy Pharmaceutical compositions effective in alleviating or reducing the effects of fatigue and weakness associated with cancer and cytotoxic cancer chemotherapy are disclosed. The pharmaceutical compositions of the present invention comprise riboflavin, effectors of the urea cycle in free form or pharmacologically acceptable salts thereof, and amino acids selected from the gorups of essential and non-essential amino acids, in free form or pharmaceutically acceptable salts thereof, suitably combined with appropriate carriers, diluents, or excipients. Also disclosed are methods of alleviating or reducing the effects of fatigue and weakness associated with cancer and cytotoxic cancer chemotherapy by administration of pharmaceutical compositions of the present invention.
CN102363619A Water soluble protoporphyrin compound and preparation method and use thereof The invention discloses a water soluble protoporphyrin compound and a preparation method and use thereof. The compound has a structure shown in the description. The water soluble protoporphyrin compound (I) or (II) disclosed by the invention has high solubility, and can form a sodium salt in aqueous solution of sodium bicarbonate and can dissolve completely. The compound has high tumor cell positioning property, high cell absorption capacity, high biocompatibility, high singlet oxygen yield as well as a bright application prospect, and can be used for photodynamic therapy in fields of malignant tumors, prostate and the like. The preparation method of the water soluble protoporphyrin is simple and easy to operate.
EP1686983B1 Use of pentadienoic acid derivates for treatement of hyperuricemia The use of a pentadienoic acid derivative of formula (I) for the preparation of a medicament for the prevention or treatment of hyperuricemia and/or one or several associated disorders or diseases, and/or for reducing the serum uric acid level of a subject. Medical compositions for these prevention and/or treatment, comprising such a pentadienoic acid derivative.
CN103520738A Carbon nano tube loaded antiviral medicine compound as well as preparation method and application thereof in production of aquaculture virus-free carrying fry The invention discloses a carbon nano tube loaded antiviral medicine compound as well as a preparation method and an application thereof in production of aquaculture virus-free carrying fries. A virus killing preparation of single-walled carbon nano tube loaded moroxydine is taken as a preparation embodiment, grass carp reovirus is taken as a testing model, a virus-free killing test is carried out on infant grass carps, and infected virus can be thoroughly killed; and due to adoption of the preparation method for aquatic fries, viruses vertically passing to children from parents can be stopped. The carbon nano tube loaded antiviral medicine compound is low in production cost and simple in use method, and can be popularized and applied tp production of specific virus free offspring fries of aquatic livestock such as fish, shrimp, crab and shellfish.
WO2009054463A1 Pharmaceutical composition containing lipophilic il-2 production inhibitor Disclosed is a pharmaceutical composition containing a lipophilic IL-2 production inhibitor and a base capable of preventing blood exposure and achieving lymphatic delivery of the lipophilic IL-2 production inhibitor through oral administration. With the use of the pharmaceutical composition, the blood exposure can be prevented for reducing side effects of the lipophilic IL-2 production inhibitor and a desired pharmacological effect thereof can be exhibited.
CN1650856A Sensitizing energistic agent of chemotherapy medicine for treating tumour A sensitizing synergist of chemicotherapeutic medicine for treating tumor is a liposoluble epigallocatechol gallate (C22H35O11-Ro).
US20080063699 Method of Administering Cationic Liposomes Comprising an Active Drug The present invention relates to the use of pharmaceutical preparations comprising paclitaxel for administration to a human patient in need thereof.
CN101181260B Rabdosia nail element clathrate and pharmaceutical preparation containing the same The invention provides an injection which takes oridonin as the treatment effective ingredient, in particular to an oridonin inclusion complex which is obtained by using the cyclodextrin inclusion technology and the injection which contains the inclusion complex. The weight ratio of the oridonin and the cyclodextrin in the oridonin inclusion complex is 1: 25 to 35. The injection which contains theinclusion complex of the invention has good stability and bioavailability, which is in line with the requirements of 'Chinese Pharmacopoeia' on preparation stability, at the same time, the inventionhas economy and practicability and the process of the invention also has good reproducibility.
EP1471899B1 Use of ambroxol in the treatment of chronic pain The invention relates to the use of ambroxol and the pharmaceutically acceptable salts thereof for producing a drug for the treatment of diseases that are caused by a strong activation of voltage-gated sodium channels, especially for the treatment of chronic pains, cerebral excitotoxicity-related disorders and cardiac arrhythmias.
US20100249198 (r)-4-(heteroaryl) phenylethyl derivatives and pharmaceutical compositions containing them The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
US20080131526 Akt sensitization of cancer cells Most human tumors find ways to resist anticancer drug monotherapy. Akt is considered a likely peptide providing such monotherapy drug resistance. Data indicates that Akt chemoresistance is induced in a p53-dependent manner and that inhibition of Akt may be an effective means of overcoming chemoresistance in cancer cells expressing wild-type p53. Breast, ovarian, lung cancer and leukemia cells lines were treated with combinations of Akt activation inhibitor Triciribine (TCN) or Triciribine phosphate (TCNP) and chemotherapeutic drugs to determine the efficiency of combination therapy. Additionally, cells were introduced into xenograft models to determine in vivo effects of combination treatment. Combining TCN or TCNP with other anticancer drugs overcame cytotoxic or treatment resistance. Thus, TCN and TCNP are shown to broaden the spectrum of human tumors that can be effectively treated.
US20100311718 Treatment of Psychoses with Dibenzothiazepine Antipsychotic The present invention provides methods for treating depression symptoms associated with bipolar disorder.
WO2006066584A1 Novel cyanoguanidine compounds Novel pyridyl cyanoguanidien compounds of general formula I (I) wherein R1, X, R2 and R3 are as defined herein, exhibit a high antiproliferative activity and may be used in the treatment of hyperproliferative and neoplastic diseases.
US20110118264 Phenyl piperazine compounds, pharmaceutical composition including the same and use thereof The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammal
US20050234222 Polypeptide comprising at least one alpha-helix having synthetically attached thereto a plurality of therapeutic or diagnostic moieties The present invention relates to a polypeptide comprising at least one alpha-helix having synthetically attached thereto a plurality of therapeutic or diagnostic moieties, wherein said therapeutic or diagnostic moieties may be the same or different and are spatially oriented on the polypeptide so as to minimise interactions between said moieties. Further aspects of the invention relate to a pharmaceutical composition comprising the polypeptide; a polynucleotide sequence encoding the polypeptide; an expression vector comprising said polynucleotide sequence; and a host cell transformed with said expression vector. The invention also provides a method of treatment comprising administering to a subject in need thereof a therapeutically effective amount of said polypeptide.
CN103638176A Medicine for treating eczema and preparation method of medicine The invention discloses a medicine for treating eczema and a preparation method of the medicine. The medicine is mainly prepared from centipede, swan-mussel, folium artemisiae argyi, calamine, buffalo horn, rosin, pepper, roughhaired holly root, gallnut and other medicines in a certain weight ratio. The medicine has the functions of clearing heat and removing toxicity, dispelling wind and relieving pain, cooling blood and eliminating edema, is quick in response and good in curative effect when used for treating eczema, and prevents relapse.
CN103381171A Applications of Chukrasone A in medicines used for treating rheumatoid arthritis The invention discloses Chukrasone A used for treating immunity inflammation. When seldane and diclofenac sodium are used as control samples, curative effect of Chukrasone A is clear in preparation of medicines used for treating rheumatoid arthritis. The applications of Chukrasone A in preparation of medicines used for treating rheumatoid arthritis is discloses for the first time. The molecular skeleton is novel, so that the inhibitory activity on rheumatoid arthritis is surprisingly strong, and it is impossible to estimate the inhibitory activity according to the inhibitory activities of other compounds. Chukrasone A possesses outstanding substantiality, and the applications of Chukrasone A in prevention and cure of rheumatoid arthritis possess significant advantages.
EP1757617A1 Ret Ligand (RetL) for stimulating neural and renal growth This invention relates to nucleotide sequences which encode a Ret ligant (RetL9, as well as to methods of stimulating neural and renal growth by treating cells and mammalian subjects with RetL DNA or protein. The invention provides a purified and isolated DNA molecule coding for a RetL, having the nucleotide sequence of any RetL, but specifically including rat retL 1 cDNA (SEQ ID NO.1), partial human RetL1 cDNA (SEQ ID NO:8), full length human retL 1 cDNA (SEQ ID NO:10), human retL2 cDNA (SEQ ID NO:12), murine retL3 cDNA (SEQ ID NO:12) or human retL3 cDNA (SEQ ID NO;16), partial human retL3 cDNA (SEQ ID NO:18) or human retL3 cDNA (SEQ ID NO:20). The invention further provides a RetL protein, with an amino acid sequence comprising that of rat RetL1 (SEQ ID NO:2), partial human RetL1 (SEQ ID NO:9), full length human RetL (SEQ ID NO: 11), human RetL2 (SEQ ID NO:13), murine RetL3 (SEQ ID NO:17), partial human RetL3 (SEQ ID NO:19) or human RetL3 (SEQ ID NO:21).
CN101703505A Special stomach medicine A special stomach medicine pertains to oral medicine for treating stomach illness, and comprises the following components by weight percentage: 60 to 75 percent of furanzolidone tablets and 25 to 40 percent of hydrochloride tablets of 2-(phenylmethyl)-1H-benzimidazole. The components are mixed and triturated, sifted by a sieve of 400 meshes, then put into a bottle and sealed for 3 to 7 days, and encapsulated with 0.1 to 0.2 gram per capsule. The medicine is taken as follows: two capsules per day, one capsule after breakfast and one capsule after supper; and one month is regarded as a course of treatment without stop. The special stomach medicine has a radical cure effect on stomach illness of the old, gastritis, chronic gastritis, superficial gastritis, gastric ulcer and gastroptosis, and has better curative effect on enteritis, colitis and duodenal ulcer compared with the existing medicine, with a total effective rate of 95 percent and a radical curative rate of more than 80 percent.
CA2383715C Improving condition of elderly pets A method is provided for improving the condition and/or increasing the longevity of elderly pets. The elderly pet is administered an effective amount of a nutritional composition which contains a calcium source and an antioxidant source, such as of vitamins or vitamin precursors which have antioxidant properties. Examples of such vitamins and precursors include 0-carotene and vitamin E.
WO2014096958A1 Inosine monophosphate and salts thereof for use in the treatment of complement-related disorders The present invention relates to the identification of novel compounds that counteract the formation of the Membrane Attack Complex (MAC) which is the terminal process during complement activation of the immune system, and that is involved in the breakdown of nerves during neurodegenerative diseases. MAC is also deposited after nerve disorders such as traumatic brain injuries and the identified compounds according to the invention are also suitable for the treatment of such disorders. The invention further relates to inosine monophosphate (IMP) and functional equivalent s thereof for use in the treatment, prevention, alleviation or inhibition of disorders mediated by undesired effects of the complement system, such as acute and chronic nerve injuries, preferably to promote axonal regeneration after such injuries have occurred.
US20080312240 Bicyclic Piperazines as Metabotropic Glutatmate Receptor Antagonists The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, Hy, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR5-mediated disorders.
CN101991632A Dropping liquid for treating cold The invention discloses a dropping liquid for treating cold, which is characterized in that each 20ml of dropping liquid contains 7-11mg of quassia extract, 0.5-0.7mg of analginum, 0.9-1.1mg of isatis root extract and 10-12mg of chlortrimeton. When in use, the dropping liquid is poured in the nasal cavity or laryngeal cavity of a patient, the treatment method is simple and special and has better effect, thus the patient is free of taking the medicine and getting an injection.
WO2014062683A1 Materials and methods for prevention and treatment of diarrhea and inflammation in the gastrointestinal tract The present invention pertains to the use of the calcium-sensing receptor (CaSR)-activating nutrients (designated as "CaSR-based nutrients") for the prevention and/or treatment of diarrheal diseases and inflammation in the gastrointestinal tract. In one embodiment, the current invention is formulated for oral administration. The anti -diarrheal composition of the present invention is useful for treating diarrheal and gastrointestinal inflammatory conditions in infants and young children.
EP1682158B9 Cosmetic compositions comprising at least a rhamnose monomer for the cosmetic treatment of skins The invention relates to a medicament comprising at least one reducing alkyl-sugar monomer having a hydroxyl function which is substituted by an alkoxy radical at C2-C40, said medicament being preferably intended to regulate inflammatory mechanisms. The reducing sugar is preferably selected from the group containing rhamnose, fucose and glucose. The invention also relates to a cosmetic treatment method involving the topical application of a composition comprising at least one reducing alkyl-sugar monomer having a hydroxyl function which is substituted by an alkoxy radical at C2-C40.
US20100022601 Sulfonamide compounds and the use The sulfoneamide compounds having the following Formula (1), which can be used as an effective component of a CaSR antagonizing agent useful for prophylaxis and/or treatment of bone disorders including osteoporosis and etc., are provided. The compounds have an excellent activity of promoting PTH secretion. In addition, the compounds are useful as an effective component of a medicament for the prophylaxis and/or treatment of bone disorders such as osteoporosis, bone fracture, hypoparathyroidism and the like.
CN103204896A 12-oxosoladulcidine amino acid conjugate, its preparation method, preparation and medical application The invention relates to the field of natural medicines and medicinal chemistry, in particular to a 12-oxosoladulcidine amino acid conjugate (I). The invention also discloses a preparation method of the 12-oxosoladulcidine amino acid conjugates, a pharmaceutical composition containing the compounds, and application of the compounds in treatment of tumor diseases or illness.
US7323474 Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase The invention relates to pyridine derivatives of formula (I) wherein the substituents and symbols are defined as indicated in the description, processes for the preparation thereof, their usage in the preparation of a pharmaceutical composition for the treatment of a disease which responds to an inhibition of angiogenesis, and pharmaceutical compositions containing such compounds.
EP2120905A1 Methods, compounds, and compositions for treating metabolic disorders and diabetes Disclosed herein are methods, compounds and compositions for preventing or treating a pancreatic disorder, including diabetes mellitus (e.g. type 1 and/or type 2 diabetes). The invention generally includes administering to a subject 1,3-propanedisulfonic acid or a pharmaceutically acceptable salt thereof, e.g., 1,3-propanedisulfonic acid sodium salt. The invention also relates to methods, compounds and compositions for improving or at least stabilizing pancreatic function(s) and for the prevention and/or treatment of metabolic syndrome and its components. The invention further relates to methods, compounds and compositions for the prevention and/or treatment of dyslipidemia, and more particularly for reducing levels of harmful serum lipid levels, especially cholesterol and triglycerides in patients in need thereof, including diabetic patients.
US6953580 Plant extracts; viricides, blood flow, alopecia The present invention provides a composition containing an extract from Wisteria floribunda, Myristica fragrans, Punica granatum, Trapa bispinosa or a derivative thereof, Coix lachiryma-jobi, Elfvingia applanata and Ganoderma lucidum or a derivative thereof (optionally further containing Panax ginseng or Panax japonicus), which has a superior antiviral activity, a superior peripheral blood flow-improving activity and a superior hair growth-stimulating activity, and a production method thereof.
US20070191428 Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E, crystalline fexofenadine free base monohydrate Form F; H1 receptor antagonist; antihistaminic drug; reduction of ketonic form, salt formation Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical compositions thereof, therapeutic uses thereof and methods of treatment therewith.
US7754751 Preferential inhibition of release of pro-inflammatory cytokines A method for preferentially inhibiting release of pro-inflammatory cytokines over release of anti-inflammatory cytokines using a fused pyrazolyl compound of formula (I): A is R or in which R is H, alkyl, aryl, cyclyl, heteroaryl, or heterocyclyl; each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is R′, nitro, halogen, —C(O)—OR′, —C(O)—SR′, —C(O)—NR′R″, —(CH2)mOR′, —(CH2)mSR′, —(CH2)mNR′R″, —(CH2)mCN, —(CH2)mC(O)—OR′, —(CH2)mC(O)H, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are —O(CH2)nO—, in which each of R′ and R″, independently, is H, alkyl, cyclyl, aryl, heteroaryl, heterocyclyl; and m is 0, 1, 2, 3, 4, 5, or 6; and n is 1, 2, or 3. This invention also covers a method of inhibiting activity of NF-κB with such a compound.
CN101530462B Composition for treating eczema and preparation method thereof The invention provides a composition for treating eczema and a preparation method thereof. The ointment is prepared by the extract or abrasive flour of corktree, the extract or abrasive flour of radix sophorae, the extract or abrasive flour of nutgall, the abrasive flours of calamine, steatite, camphol, dried alum, indigo and cinnabar, starch and teal oil. The contents of the raw materials are respectively 50-150 parts of corktree by weight, 40-80 parts of radix sophorae by weight, 15-35 parts of nutgall by weight, 100-120 parts of calamine by weight, 200-280 parts of steatite by weight, 15-25 parts of camphol by weight, 25-70 parts of dried alum by weight, 20-25 parts of indigo by weight, 5-15 parts of cinnabar by weight, and 50-100 parts of starch by weight. The preparation method mainly extracts the corktree by ethanol and extracts the radix sophorae by cooking in water. The composition in the invention for treating eczema, in particular the composition prepared by the method provided in the invention, has fast effect for treating eczema, high efficiency and high clinic cure rate, and has no easy repeatability.
EP1501359A2 Compositions comprising immunostimulatory oligonucleotides and uses thereof to enhance fc receptor-mediated immunotherapies Compositions comprising immunostimulatory oligonucleotides (CpGODN) and FcR-directed immunotherapeutics are disclosed. Also disclosed are methods of using the compositions to enhance FcR-mediated antigen presentation, ADCC, and other FcR-mediated immune responses.
CN101322727A Exterior patch for freeing collateral vessels and dispelling pain and producing method thereof The invention relates to an external patch for activating the channels and relieving pain. The patch consists of lavandula angustifolia, liquid parafin, azone, far infrared magnetic powder, red halloysite and cow milk. The production method comprises the following steps: the lavandula angustifolia is put into a container, heated slowly, added with the red halloysite and cow milk after thorough dissolution, stirred evenly and decocted with slow fire, and then added with the far infrared magnetic powder, stirred evenly, and added with the azone, continuously stirred evenly, the fire is ceased, the mixture is spread out on a fabric base with a certain specification after being cooled, thus the patch is obtained. The patch can relieve pain and numbness caused by wind cold dampness and those in joints and muscle caused by contusion and sprain, and those in the nerves compressed by the pathological changes of the vertebral body. The patch has the advantages of high adhesiveness, no odor, no irritation, no stickiness, and no side effect, feeling relaxed and free in the part with the patch. When in use, the patch is applied to the local pain spot or acupuncture point of the body, and the pain is relieved in 1-3 hours. The patch is used for hand and feet numbness caused by lumbar vertebra and cervical vertebra, the channel injury caused by the external force of the articular muscle, and the pain, swelling, coldness and numbness caused by the wind and cold in articular muscle, etc.
CA2813743A1 Selective proton coupled folate transporter and folate receptor, and garftase and/or other folate metabolizing enzymes inhibitor compounds and methods of using the same The present invention provides selective proton coupled folate transporter and folate receptor, and glycinamide ribonucleotide formyltransferase enzyme and/or other folate metabolizing enzyme inhibitors having a fused cyclic pyrimidine compound, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof. These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase and/or other folate metabolizing enzymes in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.
CN101711775B Fermentation composition for fermenting Agaricus blazei Murrill through probiotics The invention relates to influence of probiotics on antineoplastic activity of polysaccharide of edible Agaricus blazei Murrill, in particular to a method for fermenting polysaccharide of Agaricus blazei Murrill through intestinal canal probiotics to increase and improve the antineoplastic activity of the polysaccharide of the Agaricus blazei Murrill. The invention further relates to a fermentation composition prepared by fermenting the polysaccharide extract of the Agaricus blazei Murrill through the intestinal canal probiotics, and an application of the fermentation composition in preparinghealth care products or medicines for preventing and curing tumor.
CN102697776A Pharmaceutical composition with function of treating cerebrovascular diseases The invention belongs to the technical field of medicine and particularly relates to a pharmaceutical composition with function of treating cerebrovascular diseases. The pharmaceutical composition contains ozagrel sodium and 1, 3-diaza-2, 4-cyclopentadiene, wherein the weight percentage of the ozagrel sodium is more than or equal to 95 percent and less than 100 percent, and the weight percentage of the 1, 3-diaza-2, 4-cyclopentadiene is more than zero and less than or equal to 5 percent. The pharmaceutical composition provided by the invention is determined by pharmacology experiment and toxicology experiment.
CN102675311A Fluoro-acrylamide derivative The invention relates to a new compound with remarkable antibacterial and antineoplastic activity, which has the following structure (shown in formula I), and has good antibacterial function for methicillin-resistant staphylococcus aureus (MRSA) and methicillin sensitive staphylococcus aureus (MSSA) as well as good antineoplastic function for human cervical cancer Hela cells, human liver cancer BEL-7402 cells, human mucinous epidermoid lung cancer A549 cells, human breast cancer MCF-7/ s cells and human glioma U251 cells. (In the formula I,) R=-CH3 or CF3, X=O, S or N, and R1=-Cl, -F, -CH3, -CF3, -OCH3 and -OCF3.
US20120309838 Use of agomelatine in obtaining medicaments intended for the treatment of obsessive-compulsive disorder (ocd) The present invention relates to the use of agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, in obtaining medicaments intended for the treatment of Obsessive-Compulsive Disorder (OCD).
WO2006112313A1 Protective agent for retinal neuronal cell comprising indazole derivative as active ingredient As a result of an extensive study for the purpose of developing a novel medical application for an indazole derivative, it is found that an indazole derivative can inhibit the apoptosis of retinal neuronal cells induced by glutamic acid in fetal rat retinal neuronal cells, that is, an indazole derivative acts on retinal neuronal cells directly and exerts a protective effect against retinal neuronal cells. Accordingly, an indazole derivative is useful for the prevention or treatment of a ophthalmic disease associated with a retinal neuronal cell disorder or a retinal disorder.
CN102686584A Aminothiazine or aminooxazine derivative having amino linker Disclosed is a compound represented by formula (I) (wherein R1, R2a, R2b, R3, R4, R5, X, L1, L2, ring A, ring B and broken lines are as defined in the description), a pharmaceutically acceptable salt thereof or a solvate of the compound or salt, which serves as an agent for treatment of diseases that are induced by the production, secretion and/or deposition of amyloid ss protein.
US20120294942 Novel process for the preparation of roflumilast The invention relates to novel processes for the preparation of high-purity roflumilast.
CA2299366C Use of xanthophylls for improvement of duration of muscle function or treatment of muscle disorders or diseases Medicament for the prophylactic and/or therapeutic improvement of the duration of mammalian muscle function and/or treatment of mammalian muscle disorders or diseases, e.g. equine Exertional Rhabdomyolysis, comprising at least one type of xanthophylles, e.g. astaxanthin, is described. Further, the use of xanthophylles in the preparation of such medicaments, and a method of prophylactic and/or therapeutic improvement of the duration of mammalian muscle function and/or treatment of mammalian muscle disorders or diseases, are disclosed.
WO2009093916A3 Derivatives of aminoalkanols, method of obtaining aminoalkanols and their use The subject of the invention is a group of new derivatives of aminoalkaπols, more specifically [(phenoxy)alkyl]aminoalkanols and [(phenoxy)acyl)aminoalkanols, their method of obtaining and their use for production of a medicine which is used in the prophylaxis, prevention and/or treatment of diseases or symptoms having neurological background and for production of a medicine with anticonvulsant activity, which is used in seizures of various origin, also in the limbic system, in myoclonic or sound-induced seizures, in psychomotor epilepsy, as well as in relieving neuropathic or inflammatory pain.
US20100204265 Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).
WO2008026300A1 Neem seed-derived therapeutic agent for malignant tumor The object is to provide a novel therapeutic agent for malignant tumor. Disclosed is a therapeutic agent for malignant tumor or an apoptosis inducer which comprises a compound selected from epoxyazadiradione, gedunin, 17-epi-17-hydroxyazadiradione and 7-O-benzoylnimbocinol as an active ingredient.
WO2011023812A1 Microsomal prostaglandin e synthase-1 (mpges1) inhibitors A compound of formula (I): as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder selected from inflammatory diseases, nociceptive pain, auto-immune disease, breathing disorders, fever, cancer, inflammation related anorexia, Alzheimer's disease and cardiovascular diseases.
WO2008035795A1 Method for preventing and treating disease with hypochlorous acid It is intended to provide a method for preventing or treating a disease of a mammal or a bird caused by a microorganism such as a virus, a bacterium, a fungus or a protozoan as an inexpensive and simple method without fear of losing its preventive or therapeutic effect due to a viral mutation or a resistant bacterium. In the method, an aqueous solution of hypochlorous acid, which is widely used as a disinfectant in the field of prevention and treatment of diseases, approved as a food additive in the food field, and known to be secreted by neutrophils in the blood with myeloperoxidase enzyme in the medical field is used as an injection.
EP1722821A1 Composition for oral administration of tamsulosin hydrochloride and controlled release granule formulation comprising same A composition for oral administration of tamsulosin hydrochloride and a controlled release granule formulation comprising the same exhibited excellent stability and sustained release characteristics of tamsulosin hydrochloride regardless of pH changes for an extended period of time.
WO2010013768A1 Crystal of thiazolidinedione compound, and process for production thereof Disclosed is a crystal of a thiazolidinedione compound, which is useful as a peroxisome proliferator-activated receptor (PPAR) γ activator or an active ingredient for the production of an anti-cancer pharmaceutical composition. Specifically disclosed are 5-(4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H- benzimidazol-2-yl]methoxy]benzyl)-1,3-tiazolidine-2,4-dione represented by general formula (I) and a crystal of a hydrate of a dihydrochloride salt of the compound.
EP1303308B1 Aldosterone antagonist and cyclooxygenase-2 inhibitor combination therapy to prevent or treat inflammation-related cardiovascular disorders Combinations of aldosterone blockers an Cyclooxygenase-2 inhibitors useful in the treatment of inflammation are disclosed.
WO2011029415A1 Cyclobutan-1,1 -dicarboxylato complexes of platinum with n6-benzyladenine derivatives, method of their preparation and application of these complexes as drugs in antitumour therapy Cyclobutane-1,1-dicarboxylato complexes of platinum in the oxidation state +II and their crystal-solvates including the structural motif I or having the general formula Il expressed by the structural formula [Pt(cbdc)(L)2] Il or the general formula III expressed by the structural formula [Pt(cbdc)(L)(L')] III, where the symbols L and L' stand for N6-benzyladenine derivatives of the general formula IV bound to the platinum atom of the basic motif V through any adenine nitrogen atom independently chosen from the N1, N3, N6, N7 or N9 atoms, depending on the substitution rate of the molecules IV, where the substituents R1, R2 a R3 are independently chosen from the group of: hydrogen atom, halogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, cycloalkenyl, substituted cycloalkenyl, cycloheteroalkenyl, substituted cycloheteroalkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, functional group and N-R'R" group, where R' and R" independently symbolize hydrogen atom, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, cycloalkenyl, substituted cycloalkenyl, cycloheteroalkenyl, substituted cycloheteroalkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl and functional group.
WO2012062867A8 Plain pegylated liposomes for use as medicinal products for prophylaxis and therapy of haemorrhagic and thromboembolic disorders The present invention relates to plain PEGylated liposomes for use as medicinal products.
CN102784125A Cefetamet pivoxil composition freeze-dried orally disintegrating tablet and preparation method thereof The invention provides a cefetamet pivoxil composition freeze-dried orally disintegrating tablet and a preparation method thereof, relates to the technical field of medicines and medicine preparation methods, and mainly solves the problem that a cefetamet pivoxil preparation in the prior art is poor in curative effect and inapplicable to children and patients having difficulty in swallowing. The cefetamet pivoxil composition freeze-dried orally disintegrating tablet is prepared from components including, by weight, 25%-50% of cefetamet pivoxil, 25%-50% of mannitol, 2%-4% of gelatin, 0.1%-0.15% of sucralose and 42%-67% of tert-butanol-water. The cefetamet pivoxil composition freeze-dried orally disintegrating tablet prepared from the components according to the weight percent is simple in preparation process and composition, is applicable to the children and the patients having difficulty in swallowing, and has the advantages of rapidness in disintegration and effectiveness, sufficiency in medicine absorption, convenience in taking, fine taste and avoidance of the first-pass effect of livers.
CN101683341A Levobupivacaine and levisoprenaline contained frozen dry powder preparation for injection The invention relates to a levobupivacaine and levisoprenaline contained frozen dry powder preparation for injection, which takes the levobupivacaine and levisoprenaline as medical active constituentsand forms drug composite by mixing with acceptable accessories pharmaceutically. The preparation method is that: the levobupivacaine and levisoprenaline are taken as raw material, the accessories with specific kinds and proportion are added, the frozen dry powder preparation for intravenous injection is prepared and developed by adopting the illustrative technological measures; the levobupivacaine and levisoprenaline contained frozen dry powder preparation is used for treating serious difficulty in breathing, caused by bronchospasm, rapidly releasing anaphylactic shock caused by drugs and prolonging the action time of infiltration anesthesia medicines.
US20080132513 new mechanism of action, oral bioavailability and/or reduced side effects; Ca2+-release-activated Ca2+ channels inhibitors; IL-2, IL-4, IL-5, IL-13, GM-CSF, TNF- alpha , and IFN gamma inhibitors; immunosuppressant The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
US7655261 Medicament and method of treatment of patients with heavy metals A method of treatment of a diseased patient in which a dose of at least one heavy metal is delivered to the patient, with a surface area which is accessible for direct contact with the patient's tissue and effects release of heavy metal ions for uptake by immuno reactive cells. The criteria to be complied with in order for the heavy metal to be effective is that the surface area is greater than the surface area of a solid sphere of the same at least one heavy metal, and that the solid sphere and dose have the same weight. In a preferred embodiment, the dose of heavy metals is delivered to the patient as very small hollow particles.
CA2303973C Prolonged release formulation of carbamazepine The present invention provides a pharmaceutical preparation in tablet form, where the active ingredient is an anti-epileptic medication, preferably a sustained release formulation, and most preferably a sustained release formulation where the active ingredient is carbamazepine. The product consists of carbamazepine particles coated with a single hydrophobic layer and is in a disintegrating tablet form.
CN102247373A Composition of methionine vitamin B1 compound The invention relates to a composition of methionine vitamin B1 compound and a preparation thereof. The composition contains 10 parts by weight of methionine, 1 part by weight of vitamin B1, 10-40 parts of mannitol in parts by weight, wherein the vitamin B1 is dihydrate, and the parts by weight of vitamin B1 dihydrate is counted based on the vitamin B1. The preparation method of the vitamin B1 dihydrate comprises the following steps of: preparing vitamin B1 into solution with the concentration of 5-10g/100ml, then adding ethanol, wherein the proportion of the added ethanol is 20-80% of the volume of vitamin aqueous solution, stirring, and then carrying out reduced pressure distillation at the temperature of 25-85 DEG C; and carrying out vacuum drying for 1-2 hours after crystallization to finally obtain the vitamin B1 crystalline dihydrate. The invention also relates to injection of composition of the methionine vitamin B1 compound, and stability test shows that the stability of the injection is greatly improved.
WO2007034185A1 Purine compounds as hsp90 protein inhibitors for the treatment of cancer Compounds of formula (I) are inhibitors of HSP90, and of utility in the treatment of, for example, cancers: wherein ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): -X-AIk1 -(Z)m-(Alk2)n-Q (IA) wherein X is a bond, -O-, -S- -S(O)-, -SO2-, or -NH-, Z is -O-, -S-, -(C=O)-, -(C=S)-, -S(O)-, -SO2-, -NRA-, or, in either orientation -C(=O)O-, -C(=O)NRA-, -C(=S)NRA-, -SO2NRA-, -NRAC(=O)-, or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl in which one or more hydrogens is optionally substituted by fluorine; AIk1 and AIk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m and n are independently 0 or 1 , and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is cyano (-CN), fluoro, chloro, bromo, methyl, ethyl, -OH, -CH2OH, -C(=O)NH2, -C(=O)H, -C(=O)CH3, or -NH2; R3 and R4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (-CN), C1C3alkyl optionally substituted with one or more fluorine substituents, C1C3alkoxy optionally substituted with one or more fluorine substituents, -CH=CH2, -C=CH, cyclopropyl and -NH2, or R3 and R4 together represent a carbocyclic or heterocyclic ring fused to ring A, or methylenedioxy (-OCH2O-) or ethylenedioxy (-OCH2CH2O-) in either of which one or more hydrogens are optionally replaced by fluorine; Si is hydrogen, or a substituent as defined in the specification.
CN101584706A Pharmaceutical composition used for reducing blood sugar and blood fat and treating diabetes A pharmaceutical composition used for reducing blood sugar and blood fat and treating diabetes comprises the following components: berberine, asiatic cornelian cherry fruit, vitamin A, beta-carotene, vitamin B complex, vitamin C, vitamin D, vitamin E, invariable elements of calcium, magnesium and minor elements of zinc, selenium, chromium and molybdenum. The pharmaceutical composition is mainly suitable for the people suffering from high blood sugar, high blood fat and diabetes. The pharmaceutical composition is quite effective in reducing blood sugar and blood fat and treating diabetes, and can be used for a long time or applied according to the treatment course.
EP2636677A1 Cdk-inhibiting pyrrolopyrimidinone carboxamide derivative or pharmaceutically acceptable salt thereof, and pharmaceutical composition containing same as active ingredient for preventing or treating liver cell cancer The present invention relates to a CDK-inhibiting pyrrolopyrimidinone carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing same as an active ingredient for preventing or treating liver cell cancer, and the composition containing the pyrrolopyrimidinone carboxamide derivative of the present invention suppresses the cell growth of SNU-354 cell, which is a liver cancer stem cell in humans, by inhibiting CDK1 and CDK2, and induces cell apoptosis of the cell by inhibiting CDK7 and CDK 7, and thus can be effective in use for preventing or treating liver cell cancer.
WO2009074995A1 Taste masked chewable compositions of sildenafil citrate The present invention relates to chewable solid pharmaceutical compositions comprising sildenafil citrate. Sildenafil citrate is a very bitter drug, hence the conventional tablets, comprise of a film coating for aesthetic appearance and acceptability. Chewable tablets are usually uncoated and hence there is a need to mask the bitter taste of sildenafil to ensure patient acceptability. The present invention achieves the taste masking of sildenafil citrate by using an ion-exchange resin which forms a complex and masks the bitter taste of sildenafil. The ion-exchange masked sildenafil complex is then incorporated with other excipients to formulate a chewable tablet using flavours and other ingredients.
CN102225052A pH-sensitive doxorubicin nano-liposome and preparation method thereof The invention relates to a method for increasing the content of doxorubicin hydrochlorate coated by liposomes. The liposomes according to the invention comprise doxorubicin hydrochlorate, phospholipids, cholesterol, vitamin E, freeze-dried excipients, carboxymethyl chitosan, and so on. The prepared liposomes have high content of coated doxorubicin hydrochlorate, and have pH sensitivity and a long-circulation active targeting drug delivery function.
CN102429886A Indapamide osmotic pump preparation and preparation method thereof The invention discloses an indapamide monolayer osmotic pump sustained-release tablet, which comprises a tablet core and a controlled-release film coating layer, wherein the tablet core contains 0.5-2% of indapamide as a monarch drug, 1-20% of filling agent, 50-90% of penetration enhancer, 1-15% of adhesive, 1-20% of release regulator and 0.5-3% of lubricant; the controlled-release film coating layer comprises a controlled-release film forming material, a plasticizer and/or a pore-forming agent; and the filling agent comprises agar powder.
US20100183740 Potent Inhibitory Effect of Zinc in Combination with Sulforaphane on Cancer Cell Growth This invention relates to compositions comprising zinc and sulforaphane which can be used in the treatment or prevention of cancer. The invention also relates to methods of treating or preventing cancer, including prostate cancer, which comprises the administration of zinc and sulforaphane to a patient in need thereof.
CN101891704A N-(2-(2-amine)oxyethylthiobenzothiazole-6-)-2-formamide derivative as well as preparation method and applciaiton thereof The invention belongs to the technical field of chemical medicines, in particular to an N-(2-(2-amine)oxyethylthiobenzothiazole-6-)-2-formamide derivative as well as a preparation method and application thereof. The technical problem solved by the invention is to provide a novel compound for anti-tumor angiogenesis medicaments, which is the N-(2-(2-amine)oxyethylthiobenzothiazole-6-)-2-formamide derivative shown as the formula I, wherein R1 is -(CH2)nC6H5, -(CH2)nC6H5-m(CH3)m, -(CH2)nC6H5-m(CH2CH3)m, -(CH2)nC6H5-mFm, -(CH2)nC6H5-mC1m, -(CH2)nC6H5-mBrm, -(CH2)nC6H5-m(OCH3)m or -(CH2)nC6H5-m(OCH2CH3)m, n=1-8, and m=1-5; and R2 is -F, -Cl, -Br, -CxH(2x+1), -CxH(2x+1)-yFy, -CxH(2x+1)-yCly, -CxH(2x+1)-yBry, -C6H5-c(OCH3)c, -C6H5-c(OF3)c or -C6H5-c(OCH2CH3)c, x=1-8, y=1-16, and c=1-5. The derivative can be used for preparing anti-tumor medicaments.
CN102250084A Dasatinib polymorphic substance as well as preparation method and pharmaceutical composition thereof The invention discloses a dasatinib polymorphic substance. In addition, the invention also discloses a preparation method and a pharmaceutical composition of the dasatinib polymorphic substance. The dasatinib polymorphic substance disclosed by the invention has the advantages of excellent physical and chemical properties, good stability and the like, and is more suitable for industrial preparation.
WO2006021565A1 Novel substituted heteroaryloxy alkylamines and their use as monoamine neurotransmitter re-uptake inhibitors This invention relates to novel substituted heteroaryloxy alkylamines of structure (I) useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
CN103040737A Drug composition containing lansoprazole compound and preparation method of drug composition The invention discloses a drug composition containing a lansoprazole compound, which comprises the following raw materials in parts by weight: 10-20 parts of lansoprazole, 1-10 parts of edetate disodium, 1-20 parts of mannitol, 5-10 parts of sodium sulfite and 10-30 parts of sodium citrate. According to the drug composition, a pH regulator sodium citrate is screened out by a large number of tests and compounded with a stabilizing agent edetate disodium, the synergistic interaction is obvious; decrease of a pH value of strongly basic lansoprazole solution during production or a lyophilized agent during storage can be avoided well; therefore, re-dissolution of the lansoprazole lyophilized agent can be well avoided; and the solubility is good. The drug composition does not go bad and is not oxidized in a storage process, and the administration safety is ensured.
US20110230558 Use of cationic surfactants for the inactivation of toxins This invention relates to a use of a composition for the inactivation of toxins containing cationic surfactants such as ethyl-Nα-lauroyl-L-arginate HCI (LAE). It has been found that cationic surfactants such as ethyl-Nα-lauroyl-L-arginate HCI (LAE) and its salts are effective against endotoxins, exotoxins and aflatoxins.
US6924284 PARP inhibitors The present invention provides compounds comprising a bicyclic aryl moiety, such as 2H-phthalazin-1-one or derivatives thereof, compositions comprising the same, and methods for producing and using the same. In particular, the present invention provides compounds of the formula: or a pharmaceutically acceptable salt, a hydrate, a solvate, or a prodrug thereof; where Q1, Q2 and Y are those defined herein.
CN103191098A Application of sakuranetin and derivatives thereof in preparation of anti-H5N1 virus medicament The invention relates to a new application of sakuranetin and derivatives thereof in preparation of an anti-highly pathogenic avian influenza (HPAI) H5N1 virus medicament. Experiments prove that the sakuranetin and the derivatives thereof have a good inhibiting and inactivating effect. The anti-H5N1 virus medicament can be prepared by using the compounds as an active ingredient. The anti-virus medicament can be used for clinically preventing and treating influenza viruses, particularly diseases caused by HPAI H5N1 viruses. The compounds are safe, low in toxicity and strong in pharmacologic action; and the raw material sources are rich, wide and cheap, the preparation cost is low, the process is simple, and the yield is high. In order to prevent and treat the influenza viruses, particularly the HPAI H5N1 viruses, the invention provides a new medicament source, which has great practical significance and a broad application prospect in the fields of medicine and bio-pharmaceuticals, particularly in the field of preparation of anti-H5N1 virus medicaments.
US20100063038 Substituted 4-Amino-Pyrrolotriazine Derivatives Useful for Treating Hyper-Proliferative Disorders and Diseases Associated with Angiogenesis This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
US20080279789 Synergistic mixture; prophylaxis and treatment of respiratory system disorders A pharmaceutical or veterinary composition, comprises a first active agent selected from a dehydroepiandrosterone and/or dehydroepiandrosterone-sulfate, or a salt thereof, and a second active agent comprising an anticholinergic bronchodilator for the treatment of asthma, chronic obstructive pulmonary disease, or other respiratory diseases. The composition is provided in various formulations and in the form of a kit. The products of this patent are applied to the prophylaxis and treatment of asthma, chronic obstructive pulmonary disease, or other respiratory diseases.
CN100594899C Sustained release system and method for ocular delivery of carbonic anhydrase inhibitors The invention provides a device and method for treating and/or preventing raised intraocular pressure, such as that associated with glaucoma or the use of corticosteroids with adrenergic agents. The invention provides insertable sustained-release devices adapted to maintain a therapeutically effective concentration of one or more adrenergic agents for an extended period of time, and a method of use thereof.
US20090227674 Combination methods fo saha and targretin for treating cancer The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of SAHA or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of Targretin. The SAHA and Targretin may be administered to comprise therapeutically effective amounts.
US20080275040 8-(1-Piperazinyl)-Quinoline Derivatives and Their Use in the Treatment of Cns Disorders This invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.
WO2012082013A3 Pharmaceutical composition for stimulating the regeneration of supporting tissue and articular cartilage (variants) The invention relates to the field of medicine and pharmaceutics and, more specifically, to the creation of a pharmaceutical composition in the form of a suspension for the prevention and treatment of problems in the physiological and reparative regeneration of tissues of the musculoskeletal system, namely bone tissue and articular cartilage. The pharmaceutical compositions for stimulating the regeneration of supporting tissue and articular cartilage contain a substance called "Mitsellat of calcium carbonate and magnesium". Research shows that the proposed pharmaceutical compositions have a marked specific pharmacological effect, exhibiting a reparative and regenerative effect with respect to bone tissue in animals, and do not have a marked general toxic effect in different doses and routes of administration to laboratory animals. The compositions do not exhibit an irritant effect, and no sensitizing effect has been observed. The proposed pharmaceutical compositions are effective and safe and can be used to prevent and treat problems in the physiological and reparative regeneration of tissues of the musculoskeletal system, inter alia in diabetes mellitus patients.
WO2013117683A1 New pediatric uses of cabazitaxel The present invention relates to the compound of formula (I): which may be in the form of an anhydrous base, a hydrate or a solvate, for its use for the treatment of pediatric cancers.
US20050085415 Nanoparticles injected directly into eye; integrin receptor antagonist; angiogenesis inhibitor, polypeptide Method and compositions for prophylaxis and/or treatment of diseases of the eye using antagonists of the integin receptors αvβ3 and/or αvβ5. The compositions can be nanoparticles and are administered to the eye by injection into the subTenon's space of the eye.
US8168193 Molecules, compositions, methods and kits for applications associated with flaviviruses A method for controlling a flavivirus entry into a cell, kits for assaying the flavivirus entry into the cell, and methods of treating and preventing flaviviruses infections are disclosed, together with vaccine and pharmaceutical compositions.
WO2014086994A1 Hsp for use in treatment for imiquimod related side effects The invention relates to a healthcare product comprising (i) a component selected from the group of heat shock proteins from alfalfa and heat shock protein hydrolysates from alfalfa, the product further comprising imiquimod or a pharmaceutically acceptable salt or derivative thereof. Further, the invention relates to a healthcare product for use in the prophylactic or therapeutic treatment of a skin disorder. Further, the invention relates to HSP for use for use in preventing the occurrence of a negative-side effect of a treatment with imiquimod, or alleviating such side effect.
US20090088401 In-situ cancer autovaccination with intratumoral stabilized dsRNA viral mimic An improved autovaccination method designed to prevent or treat various neoplastic diseases by inducing a systemic immune response against a tumor and its remote metastases, consisting of the induction of an immunogenic cell death in one or more targeted tumor sites with local radiation therapy, cryotherapy, heat, chemotherapy or various other treatments, followed by intratumoral/peritumoral injection of dsRNAs (poly-ICLC in particular) in the same tumor site.
US20060034911 New oral immediated release dosage form The present invention relates to a solid oral immediate release dosage form of a pharmaceutically active compound, N-[(1,2,3,4-tetrahydro-5-methyl-8-(4-methylpiperazin-1-yl)-2-naphthyl]-4-morpholinobenzamide, in the form of the free base or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing said dosage form, the use of said dosage form and a method of prevention and/or treatment of CNS disorders and related medical disturbances using said dosage form.
US6916834 Preparations and use of an Ah receptor ligand, 2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester Preparation, use, and structure of endogenous Ah receptor ligand is disclosed.
WO2010087313A1 Neurite elongation stimulator Disclosed is a novel neurite elongation stimulator. The neurite elongation stimulator comprises a compound represented by general formula (1) as an active ingredient. In general formula (1), R1 to R3 independently represent a hydrogen atom or a proper substituent; Z1 represents a heterocyclic ring, and Z2 represents a heterocyclic ring which is the same as or different from the heterocyclic ring represented by Z1, or an aromatic ring, wherein each of the heterocyclic ring and the aromatic ring may have a substituent; o represents an integer of 0, 1 or 2, and p represents an integer of 0 or 1, wherein p is 1 when o is 0 or 2, p is 0 when o is 1, R1 and R2 do not exist when o is 0, and R3 does not exist and a carbon atom to which R2 is bound and Z2 are bound to each other through a single bond when p is 0; X1 - represents a proper counter anion; and q represents an integer of 1 or 2.
EP1713776B1 Quinoline derivatives for use as mycobacterial inhibitors The present invention relates to novel substituted quinoline derivatives according to the general Formula (I), useful in the treatment of mycobacterial diseases such as TB.
CN1814151A Medicinal granules of nourishing Yin and tonifying stomach, capsule and tablet preparing method The invention relates to a method for preparing micron Tang-Shen-Lv-Hou-Wang- Xi-Tian-Dou-Feng-Jiao granules, capsules and tablets for nourishing Yin and the stomach, prepared of micron genseng whisker powder, micron coppper and sodium chlorophyllide powder, micron Filamentous Fungi powder, micron West ginseng powder, micron Radix Asparagi powder, micron O.Dendrobium Candidum Wall.et Lindl powder, Royal Jelly Powder, Bee Pollen Powder, oligosaccharide powder, etc, manufactured by high-tech airflow superfine crushing, having obvious functions of nourishing Yin and the stomach, improving immunity, etc, able to make the middle-aged and aged patients with stomach trouble obtain hundreds of rich nutrient substances, such as vitamins, and chlorophyll, reinforcing the health functions of nourishing Yin and the stomach and facial beautifying and maintaining, and thus having the features of China.
WO2012155827A1 Use of indole-2,3-dione in preparing medicine for improving dyszoospermia The present invention relates to the use of indole-2,3-dione in preparing medicine for improving dyszoospermia. The indole-2,3-dione is natural product or artificially synthesized product. It is less toxic, and causes fewer side effects. The indole-2,3-dione plays a good role in improving dyszoospermia and promoting fertility.
US7109203 for use in the treatment or prevention of diseases in which bradykinin B1 receptor activation plays a role Sulfonamide derivitives of the formula I wherein R1-R6 are as defined in the description, processes for their production, their use as pharmaceuticals, particularly for use in the treatment or prevention of diseases in which bradykinin B1 receptor activation plays a role or is implicated, and pharmaceutical compositions comprising them
WO2011024955A1 Nucleic acid capable of binding to tgf-βii-type receptor, and use thereof Disclosed is a substance which can be used for the elucidation of the physiological functions of TGF-β and a TGF-βII-type receptor and the analysis of mechanism of development of TGF-β-induced diseases and the diagnosis and treatment of TGF-β-induced diseases. Specifically disclosed are: an aptamer which is characterized by being capable of binding to a TGF-βII-type receptor and being capable of inhibiting the binding between TGF-β and a TGF-βII-type receptor; a method for detecting a TGF-βII-type receptor, which is characterized by using the aptamer; a medicinal agent comprising the aptamer; and others.
WO2014139882A1 Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseasesby administering the compound of the invention.
CN101269045A Galantamin hydrobromide sustained-release dropping pill and preparation method thereof The invention discloses a drug compound oral pharmaceutical preparation used for treating myasthenia gravis and sequela of poliomyelitis and for resisting the effect of non-depolarized muscle relaxation of intocostrin and similar drugs, and particularly relates to a sustained-release galanthamine hydrobromide dropping pill used for treating syphilis, gonorrhoea and chlamydia or mycoplasma infection. The pharmaceutical preparation aims to supplement the deficiency of the prior art and provide a sustained-release galanthamine hydrobromide dropping pill. The sustained-release galanthamine hydrobromide dropping pill can overcome the defects in the prior art effectively, guarantee no occurrence of an obvious quality change for the drug during the effective storage period and have the advantages of controllable release time, full release and high bioavailability simultaneously.
WO2007029361A1 Sustained-release microsphere containing short chain deoxyribonucleic acid or short chain ribonucleic acid and method of producing the same It is intended to provide a sustained-release microsphere preparation containing a short chain deoxyribonucleic acid or a short chain ribonucleic acid as the active ingredient which has been improved in the sustained-release properties and remains efficacious over a long period of time. It is intended to provide a microparticle preparation having a short chain deoxyribonucleic acid or a short chain ribonucleic acid stably encapsulated therein which can regulate the expression of a specific protein relating to a disease over a long time and can be injected or transmucosally administered, and a method of producing the same. A sustained-release microsphere (in particular, a sustained-release microsphere prepared via a w1/o/w2 type emulsion)preparation containing a short chain deoxyribonucleic acid or a short chain ribonucleic acid (in particular, an SiRNA) as the active ingredient, characterized by containing a positively charged basic substance such as arginine, polyethyleneimine, a cell-permeable peptide, poly-L-lysine or poly-L-ornithine in a biodegradable polymer.
DE102004031538A1 Presentation form (obtainable by dissolving indibulin in or with a highly concentrated organic acid), useful to orally administer poorly soluble active compound indibulin, comprises a poorly soluble active compound indibulin Presentation form (A) comprises a poorly soluble active compound indibulin (in the form of a supersaturated solution) for oral administration; where (A) is obtainable by dissolving indibulin in or with a highly concentrated organic acid (which is physiologically tolerable per se in diluted form), and diluting by adding water to a physiologically tolerable concentration of the organic acid. Independent claims are also included for: (1) the preparation of (A); and (2) a kit for the simplified handling of the preparation of (A). - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : Tubulin inhibitor.
CN101015558A Preparation of superfine prednisolone powder This invention relates to a method for preparing superfine prednisolone powder, and belongs to the field of micronization. Open question at present: particle diameter of prednisolone is small but can not obtain dry powder, or the dry powder has wide size distribution, bad redispersibility, and instability in water. The invention is to realize the preparation of prednisolone granule with controllable particle diameter, narrow particle size distribution, and superfine or nano-graded quadrilate and hexagon through inverse solvent recrystallization.the prednisolone of the invention has the advantages of controllable particle diameter, narrow particle size distribution, good redispersibility, stable micropowder, and good dissolving effect; and has prodigious dominance in the development of drug effect and new medicament form.
EP1869053A1 Substituted 4,5,6,7-tetrahydro-isoxazolo[4,5-c]pyridine compounds and their use in the production of medicaments The invention relates to substituted 4, 5, 6, 7-tetrahydro-isoxazolo [4, 5-c] pyridine compounds of formula (I), to a method for their production, to medicaments containing said compounds and to the use of said compounds for producing medicaments. It has been found that substituted 4,5,6,7-tetrahydro-isoxazolo[4,5-c] pyridine compounds of general formula (I) are suitable for noradrenaline receptor regulation, in particular for inhibiting the noradrenaline (NA) uptake, for 5-HT receptor regulation, in particular for inhibiting the 5-hydroxy-tryptophan (5-HT) uptake and/or for batrachotoxin (BTX) receptor regulation and can thus be used in particular as pharmaceutical active ingredients in medicaments for the prophylaxis and/or treatment of disorders or diseased that are associated with said receptors or processes.
EP2651894A1 Thiosemicarbazone compounds and use in the treatment of cancer The present invention relates to dipyridyl thiosemicarbazone compounds of formula (I): wherein R1 is cyclohexyl or ethyl; as well as pharmaceutical compositions containing those compounds, and the use of those compounds and compositions in the treatment of cancer.
WO2010097371A1 Ceramide-analogous metabolites This invention relates to certain ceramide-analogues of FTY720 (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol; fingolimod). In particular, the present invention relates to pharmaceutical compositions comprising these compounds, as well as processes for their preparation and their use in the treatment of autoimmune conditions, such as multiple sclerosis.
CN101104643A Polysaccharide sulfate selenide compound and its preparation method and application Disclosed are a selenium polysaccharide sulfate compound and a preparation method and applications of the selenium polysaccharide sulfate compound, belonging to the polysaccharide selenide technical field. The selenium polysaccharide sulfate compound is characterized in containing pyran sugar units or/and furan sugar units. The preparation method adopts reaction between polysaccharide sulfate and selenide reagent which is selenous acid and selenite. Molar ratio of the selenide reagent and groups of the polysaccharide sulfate is 1: 0.1-10. The compound of the invention is applied in preparing anticancer drug and ant-oxidation drug. The polysaccharide selenide sulfate of the invention is produced by substitution reaction between selenous acid and sugar unit sulfate radicals. Therefore, the yield and the quality of the product are both higher than that of the product produced by other methods. The invention also has advantage of high selenium content: the highest content of the selenium can reach to 45 percent which is much higher than 12.5 percent reported in literature.
US20120288553 Method for controlling toxicity of metallic particle and low-toxicity composite of metallic nanoparticle and inorganic clay The present invention provides a method for controlling toxicity of metallic particles and a low-toxicity composite of metallic nanoparticles and inorganic clay. The metallic nanoparticles are effective in preventing infection and in skinning over, and thus suitable for treating scalds/burns. In the composite, the weight ratio of metallic nanoparticles to inorganic clay preferably ranges 0.1/99.9 to 6.0/94.0 in a size of about 5 to 100 nm. Preferably, the metal is silver and the inorganic clay is nano silicate platelets.
EP2655345A1 Aryl triazole compounds with antitumoural activity The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical composition containing such compounds.
EP1847269A1 Utilisation of acetyl salicylic acid (ASA) when using a membrane lung Use of acetyl salicylic acid (I) in the manufacture of a medicine, which can be administered through a lung membrane to a human, to avoid or minimize the deposition of the blood components in the lung membrane, where, in the beginning, (I) is administered once daily, many times or continually and within the risk range for its analgesic effect. - ACTIVITY : None given. - MECHANISM OF ACTION : None given.
WO2007132179A3 Therapeutics comprising pyridinium derivatives The present invention relates to the use of a compound of formula (1) wherein: R1 comprises a carbonyl group and R2 is a hydrocarbyl group; optionally wherein said ring is further substituted; or a pharmaceutically acceptable salt thereof; in the manufacture of a medicament for use in one or more of: modulating the release of intracellular calcium from a store controlled by nicotinic acid adenine dinucleotide phosphate; modulating calcium spikes in mammalian cells; treating diseases in one or more of brain, heart, pancreatic cells (e.g. pancreatic acinar and pancreatic beta cells), immune cells, T-cells, haemopoietic cells including phagocytes; treating diseases in one or more of brain, heart, pancreatic cells (e.g. pancreatic acinar and pancreatic beta cells), immune cells, T-cells, haemopoietic cells including phagocytes by modulating the release of intracellular calcium from a store controlled by nicotinic acid adenine dinucleotide phosphate; treating diseases in one or more of brain, heart, and T-cells by modulating calcium spikes in mammalian cells.
CN102846597A Medicinal use of artemisinin and artesunate against alzheimer disease The invention relates to the field of natural medicaments, and in particular relates to a medicinal use of artemisinin and artesunate against alzheimer disease. Researches find that artemisinin and artesunate have the effects on inhibition of generation of Abeta 42, and Ic50 is in the range of 1.6-4.0 mu m. Molecular weights of artemisinin and artesunate are less than 500 Daltons, and mean that the compounds have the potential capability of permeating brain-blood barriers, more importantly, artemisinin and artesunate do not affect cytotoxicity and cell apoptosis in the range of inhibiting the concentration of Abeta 42, and do not have side effects on a Notch signal path.
US20100310635 Compositions and Methods for Regulating T-Cell Activity Methods, compositions and kits effective for modulating and immunomonitoring of Treg activity are provided. Therapeutic methods involving formation and uses of cleaved Foxp3 are disclosed, as well as screening assays for identifying agents effective for modulating Treg activity.
WO2007149728A3 Aryl and heteroaryl tetrahydrobenzazepine derivatives and their use for treating glaucoma Aryl tetrahydrobenzazepine derivatives with minimal 5-HT2B activity relative to 5-HT2A and 5-HT2C activity that are useful for treating glaucoma are disclosed.
CN101884622B Benserazide sustained-release microspherical composition and preparation method thereof The invention relates to a benserazide sustained-release microspherical composition, which comprises the following components by weight percent: 40%-99% of a degradable hydrophobic polymer and 1%-60% of benserazide. The invention also provides a preparation method of the benserazide sustained-release microspherical composition. The invention can overcome the instability of benserazide during the storage process and improve the pharmaceutical therapeutic effect on patients. The method for preparing the microspherical composition can avoid the defects of low entrapment rate of the conventional W/O and W/O/W, and environmental pollution of S/O/O caused by serious burst release. In the invention, the grain diameter of the microspherical composition prepared by the method can be controlled according to different demands without environmental pollution, and the influence on the therapeutic effect of benserazide can be prevented. The surfaces of the obtained granules are smooth and rounded, the granules are regular without adhesion, the grain diameter can be regulated and controlled from 1mum to 5mum as required, and freeze-drying powder of the granules is white, exquisite and loose, is not collapsed and adhered, and has good redispersibility.
CN101259181A Preparation of qinkailing freeze-dried injection The invention provides the preparation method of the freeze-dried powder injection of qingkailing, which is prepared by cholic acid, nacre, hyodeoxycholic acid, gardenia, buffalo horn, isatis root, baicalin and honeysuckle, which undergo the processes of extraction, alternative precipitation and multipole impurity removal to obtain extraction solution in which absolute ethyl alcohol is added. Compared with prior art, the invention increases the content of effective composition of the medicine, shortens the time of freeze drying, reduces production cost and optimizes processing technique. In addition, the examinations of insoluble particle and visible matter are greatly improved, so the bioavailability and stability of the medicine are improved. The preparation of the freeze-dried injection of qingkailing has the advantages of loose texture, good formability, low water content, good stability, and good appearance and color, reducing insoluble particles and being easy to store, so the clinical curative effect of the preparation can be ensured.
WO2012093741A1 Leukaemia-treatment pharmaceutical composition The present invention relates to a leukaemia-treatment pharmaceutical composition, and more specifically to a Myc protein activity inhibitor comprising a 4-quinolinone derivative and to a cancer-treatment pharmaceutical composition which uses the 4-quinolinone derivative as an active ingredient, wherein the leukaemia-treatment pharmaceutical composition according to the present invention suppresses Myc/Max/DNA complex formation and so induces cell cycle arrest, thereby giving the advantage that the composition can suppress the growth of various human leukaemia cell strains, and can advantageously be used to prevent and treat leukaemia.
WO2010129318A2 Topical compositions comprising an alkoxylated diphenylacrylate compound and an organic nonionic emulsifier A topical composition of improved spreadability and aesthetical appeal is provided, which contains a stable emulsion base formed by combining an alkoxylated diphenylacrylate compound and a nonionic organic emulsifier with a pharmaceutically or cosmetically acceptable carrier. Preferably, the topical composition is a sunscreen composition that further contains inorganic or physical sunscreen agents dispersed in such a stable emulsion base, which is characterized by improved photo-protection of the skin and is effective in preventing/reducing photo-damage of the skin upon exposure to sunlight or other sources of light in the ultraviolet (UV), visible, and infrared (IR) ranges.
US7816403 Administering a thiuram disulfide and a heavy metal ion; activated transcription factor/adenosine cyclic phosphate response element binding protein (atf/creb) There is provided a method for inhibiting ATF/CREB and cancer cell growth using disulfiram, administered in combination with heavy metals. It was found that disulfiram disrupts transcription factor DNA binding by forming mixed disulfides with thiols within the DNA-binding region, and that this process is facilitated by metal ions. Disulfiram administered to melanoma cells in combination with copper (II) or zinc(II) decreased expression of cyclin A, reduced proliferation in vitro, and inhibited growth of melanoma cells. The combination of oral zinc gluconate and disulfiram at currently approved doses for alcoholism stabilized tumor growth in two of three patients with Stage IV metastatic melanoma, with 12 and 17 month survivals, respectively, to date, and produced a >50% reduction in hepatic metastases in one individual.
CN102247360A New application of 3,3'-diindolylmethane The invention belongs to the field of radiation injury protective medicaments, and relates to new application of 3,3'-diindolylmethane, namely application to the preparation of the radiation injury protective medicaments. A structural formula of the 3,3'-diindolylmethane is shown in the specifications. The 3,3'-diindolylmethane can be used for preparing the radiation injury protective medicaments and can improve the survival rate of cells subjected to ionizing radiation under the condition of low concentration without toxic or side effect.
US7122678 (Trans)-(3,4-Dimethyl-cyclopentyldine)-acetic acid ethyl ester; treating epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, irritable bowel syndrome (IBS), and inflammation The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
US20080312327 Organic Compositions Provided is an improved liquid composition for the treatment of surfaces, preferably the skin and/or hair in order to provide a cleaning and/or sanitizing effect thereto, which necessarily comprises: one or more detersive surfactants selected from anionic, nonionic, cationic, and amphoteric surfactants; a first biocidal constituent(s) which provide a biocidal effect in conjunction with at least one or more second biocidal constituent(s) selected from benzoic acid, benzoic acid derivatives and salts thereof or farnesol, one or more pH adjusting constituents, optionally one or more organic solvents, hydrotropes, and further additive constituents, and water. In preferred embodiments the hydrotrope and/or organic solvents are desirably excluded from the compositions, and the composition is thickened. The compositions are particularly useful as a hand wash composition, body wash or shampoo.
US20120322821 Ghrelin receptor agonist for treatment of cachexia The present invention relates to use of a compound of the present invention or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, for the manufacture of a medicament for the treatment of cachexia. The invention also relates to a method for the treatment of cachexia, comprising administering the compound of the present invention or a pharmaceutical composition comprising the same to a human or an animal. The invention further relates to use of said compound, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, in combination with one or more second active agents. Moreover, the invention relates to a pharmaceutical composition and a kit comprising the compound of the present invention or a pharmaceutically acceptable salt thereof, for the treatment of said disease.
US20080234354 Administering (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane alone or in combination with a second antiappetite or antiobesity agent; treating or preventing disorders related to or complicated by obesity The present invention provides novel compositions and methods for the controlling appetite and weight and/or treating obesity using a (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or related compound. The invention also provides novel compositions and methods for treating or preventing disorders related to or complicated by excessive body weight or obesity, including coronary heart disease, osteoarthritis, osteoporosis, dislipidemias, gout, atherosclerosis, joint pain, sexual and fertility problems, respiratory problems, gall bladder disease, skin conditions, hypertension, diabetes, stroke, pulmonary embolism, sleep apnea, idiopathic intracranial hypertension, lower extremity venous stasis disease, gastro-esophageal reflux, urinary stress incontinence, metabolic syndrome, insulin resistance and cancer. The methods and compositions of the invention may employ a (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or related compound alone, or in combination with a second anti-appetite or anti-obesity agent.
CN103070884A Composition for treating dog enterogastritis The invention belongs to the field of veterinary medicines, and particularly relates to a composition for treating dog enterogastritis. The composition comprises gentamicin and egg white with a mass part ratio of 1:6-1:10, preferably 1:8. The composition has a better synergistic effect by combining the gentamicin with the egg white, and is remarkable in treatment effect of the dog enterogastritis and low in cost.
CN101199765A Medicament for treating stomach disease Disclosed is a medicine for treating gastritis. The invention is prepared by the raw materials with the following weight proportions: Taibaimi(bulb of Notholirion hyacinthinum) 2-20, Radix Astragali 8-35, Rhizoma Dioscoreae Bulbiferae 5-30 and Rhizoma Corydalis 5-25. The preparation process is that the Rhizoma Corydalis is dried, crushed and is filtered through a 100mesh sieve to form powder 1 for later use; the Taibaimi(bulb of Notholirion hyacinthinum), Radix Astragali and Rhizoma Dioscoreae Bulbiferae are extracted for two times in water 5-20 times of the total weight of the three, and the extraction each time costs 1.5 hours; the extractives are mixed, condensed and dried to form powder 2; the dregs of the decoctions are further extracted in hydrophilic organic solvent, the rate of the dregs and the organic solvent is 1: 4-20, the dregs are dissolved for 1-8 hours in the solvent under the temperature between 20 DEG C - 120 DEG C and are extracted for two times with each time 1-5 hours, then the extractives are cooled under the room temperature and filtered, the residues are filtered out, the filtered liquid is condensed and the organic solvent is recovered, and then the condensed liquid is dried under 80 degrees to form a solid product 3; the products 1, 2 and 3 are combined together to be taken as the effective ingredients and then mixed evenly and prepared into granules which are encapsulated. The invention mainly treats acute and chronic gastritis, superficial gastritis, atrophic gastritis, gastric and duodenal ulcer, early stage of gastric cancer and esophagus cancer.
CN102159221A Anti-infective formulation and methods of use The present invention relates to a formulation for administration to the teat canal or/and lower portion of teat cistern of a mammary gland of an animal, wherein the formulation prior to delivery is in the form of a paste, the formulation including: an oil-based physical barrier material which is able to form a cohesive mass in the teat canal and/or the lower portion of the teat cistern, and at least one antiseptic compound mixed with the barrier material.
CN102153575A Dioxane-coordinated rare-earth coordination compound, and preparation method and application thereof The invention provides a rare-earth fluorescent coordination compound synthesized by using dioxane micromolecule as a second ligand and pipemidic acid (PPA) as a first ligand, and a preparation method thereof. Due to the existence of dioxane, the fluorescence of the rare-earth coordination compound is obviously enhanced, and the fluorescence lifetime of the rare-earth coordination compound is greatly influenced when the dioxane is used as the second ligand. The novel rare-earth coordination compound provides a new optional reagent for quinolone broad-spectrum antibacterial drugs, and the fluorescence enhanced phenomenon also provides a new method for detecting existence and content of micromolecule dioxane.
WO2014157137A1 Oral administration preparation with masked bitterness of silodosin Provided is a novel oral administration preparation that allows a subject to easily take, even without water, silodosin that is a highly bitter drug without getting a feeling of strangeness and has such dissolution properties as to re-achieve a blood silodosin concentration effective for treating dysuria, etc. caused by prostatic hypertrophy. The present invention relates to masking grains, said masking grains being prepared by granulating drug grains that contain micropowdery silodosin using a coating agent that contains a non-enteric polymer or coating the drug grains with the coating agent, wherein the content of the non-enteric polymer is 80-400 parts by mass per 100 parts by mass of silodosin, a novel oral administration preparation comprising the masking grains, etc.
US20110002970 Process for the preparation of nano zinc oxide particles A process for the preparation of nano zinc oxide particles comprising dissolving a zinc metal precursor in a solvent to obtain a first solution; dissolving a base in an alcohol to obtain an alkali solution; and adding the alkali solution to the first solution over a predetermined period of time to obtain nano zinc oxide particles in solution.
EP2336127A1 Tiotropium salts, method for creating same and medicinal formulations containing same Tiotropium salts, their solvates and hydrates are new. Tiotropium salts of formula (I), their solvates, hydrates are new. [Image] X ->anion. Independent claims are included for the following: (1) a pharmaceutical composition (C1) comprising (I) and carrier or excipient; and (2) preparation of (I). - ACTIVITY : Respiratory-Gen.; Antiasthmatic. - MECHANISM OF ACTION : None given.
EP2548558A1 Nitrogen-containing condensed heterocyclic as inhibitors of bruton's tyrosine kinase Described herein are irreversible kinase inhibitor compounds having the structure: wherein: is an active site binding moiety selected from Y is a linker moiety and G is a Michael acceptor moiety; methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
CN102198184A Effect of morinda officinalis extract on improving or treating sexual disorder, and application thereof The invention relates to the effect of a morinda officinalis extract on improving or treating sexual disorder, and an application thereof. The substance for treating or improving the sexual disorder has an effect on integrally regulating the hypothalamus, the pituitary gland, the sex gland and the adrenocortical function to improve or treat the sexual disorder, and simultaneously has selective specificity on different 5-HT receptors, i.e., the substance can selectively excite the 5-HT1 receptor, but has no excitation on the 5-HT2 receptor and the 5-HT3 receptor. The morinda officinalis extract can be used as a medicament and/or food for treating or assisting to improve the sexual disorder.
EP1951739A1 An improved process for the isolation of arjunic acid from the bark of the tree terminalia arjuna and the use of this compound in the treatment of cancer The present invention provides an improved process for the isolation of oleane compounds from the bark of Terminallia arjuna ( Roxb.). More particularly, the present invention relates to an improved process for the isolation of arjunic acid and its derivates from the bark of Terminallia arjuna ( Roxb.). The present invention further provides the identification of arjunic acid [1] and its derivatives as anticancer agent useful in the treatment of various types of cancer in humans.
CN103429583A Triazole derivatives as WNT signaling pathway inhibitors The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear ss-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.
US20120046357 Benzamide and Napthamide Derivatives Inhibiting Nuclear Factor-Kappa (B) - (NK-kB) The invention relates to compounds of formula (1) and formula (2), and pharmaceutically acceptable salts thereof for the treatment of cancer, inflammation, auto-immune diseases, diabetes and diabetic complications, infection, cardiovascular disease and ischemia-reperfusion injuries, wherein R1 is defined herein.
US20100003225 Hsp60, hsp60 peptides and t cell vaccines for immunomodulation The present invention provides novel uses for peptide p277—positions 437-460 of human heat shock protein 60 (HSP60)—in modulation of immune responses and inflammatory diseases. The invention further provides novel uses for HSP60 and p277 in the treatment or prevention of hepatic disorders. The invention discloses methods for treating, preventing or ameliorating the symptoms of T cell mediated inflammatory and autoimmune disorders, including hepatic disorders, which comprise administering to a subject in need thereof a composition comprising as an active ingredient an effective quantity of a molecule selected from: HSP60, p277, fragments, analogs, homologs and derivatives thereof, and nucleic acids encoding same. Also disclosed are T cell vaccination methods for treating or preventing T cell mediated disorders.
CN102451170A Granisetron hydrochloride freeze-drying tablet and preparation method thereof The invention relates to a granisetron hydrochloride freeze-drying tablet, and a prescription and a technology for preparing the granisetron hydrochloride freeze-drying tablet by a lyophilization method. The granisetron hydrochloride freeze-drying tablet is prepared from a main drug of granisetron hydrochloride and pharmaceutic adjuvants. The granisetron hydrochloride freeze-drying tablet can be administered without water and disintegrate immediately after entering mouth, and is suitable for the elder and children patients that have difficulty in swallowing; the granisetron hydrochloride freeze-drying tablet has advantages of convenient administration, fast absorption, small first pass effect and mall excitant to alimentary canal mucous membrane and has wide market application prospect; as no water is needed during administration, symptoms of nausea and vomit will not be aggravated; therefore, the granisetron hydrochloride freeze-drying tablet has better compliance and treatment effect than other dosage forms on nausea and vomit caused by chemotherapy, radiotherapy or operation and can obviously reduce side-effect of granisetron hydrochloride. In addition, the invention also relates to a preparation method of the granisetron hydrochloride freeze-drying tablet.
US20090264509 Adenoviral vector-based foot-and-mouth disease vaccine The invention is directed to an adenoviral vector comprising at least one nucleic acid sequence encoding an aphthovirus antigen and/or a cytokine operably linked to a promoter. The adenoviral vector is replication-deficient and requires at most complementation of both the E1 region and the E4 region of the adenoviral genome for propagation. The invention also is directed to a method of inducing an immune response in a mammal comprising administering to the mammal a composition comprising the aforementioned adenoviral vector.
CN103370316A 3-aryl-6-aryl-[1,2,4]triazolo[4,3-a]pyridines as inhibitors of cell proliferation and the use thereof Disclosed are 3-aryl-6-aryl-[1,2,4]triazolo[4,3-a]pyridines thereof, represented by the Formula (I), wherein Ar1, Ar2, R1-R3 are defined herein. Compounds having Formula (I) are inhibitors of cell proliferation. Therefore, compounds of the invention may be used to treat clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
WO2008097546A2 Compounds that inhibit cholinesterase Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.
CN102218088A Oral ulcer inunction liquid An oral ulcer inunction liquid. The invention relates to a medicament, and especially relates to an oral ulcer inunction liquid for treating oral ulcer. A technical scheme of the invention is as follows: 1. a formula proportion of the invention is that, by weight, menthol 5-15, borneol 5-15, dimethyl sulfoxide 8-12, salicylic acid 20-30, glycerin 20-30, 75% alcohol 300-500 and distilled water 10-30; 2. preparation process comprises the steps of: mixing and dissolving menthol, borneol, dimethyl sulfoxide, salicylic acid, glycerin; adding into the 75% alcohol after complete dissolving; mixing uniformly and adding distilled water; shaking well to finish. The present invention has the beneficial effects that: compared with similar paste agent, powder, lozenge and pad pasting for treating oral ulcer, the oral ulcer inunction liquid has faster curative effects, good pain relieving effect, rapid effectiveness after application, and oral ulcer surface can be healed within 3-4d.
CN101785786B Chlorine dioxide ointment used for treating dermatophytosis The invention relates to a chlorine dioxide ointment used for treating dermatophytosis, which comprises the following compositions by weight percentage: 1-50 parts of bactericide precursor, 10-100 parts of emulsifier, 100-400 parts of skin care grease, 0.5-20 parts of chelant, 1-40 parts of hygroscopic agent, 1-60 parts of thickening agent and 1000 parts of purified water. The ointment is suitable for treating various types of skin fungus infection and is particularly applicable for the patient who is not recovered by adopting other medicines; the patient administrates the ointment once everyday and can be recovered after the sustained administration for one week, and the recovery rate is 100% without recurrence.
EP1575960B1 1,4-diazabicyclo 3.2.2 nonanecarboxamide derivatives, preparation and therapeutic use thereof The invention concerns compounds of general formula (I), wherein: X represents a nitrogen atom or a group of formula C-R2; P represents a group of formula C-R3; Q represents a group of formula C-R4; R represents a group of formula C-R5; W represents a group of formula C-R6; or one among the symbols P, Q, R and W represents a nitrogen atom; R1 represents a hydrogen atom or an alkyl group; R2 represents a hydrogen atom or an alkyl group; R3, R4, R5 and R6 represent each a hydrogen or halogen atom, or an alkyl, alkoxy, nitro, amino, trifluoromethyl, cyano, amino group or other functional groups. The invention is applicable in therapeutics.
US20060141580 Encoding protein with immunomodulatory activity, antiviral activity, and antitumor activity; treating any Type 1 interferon treatable disease including cancer; determining if a patient will respond to interferon treatment; transgenic animals The present invention relates to identification of a gene upregulated by interferon-α administration corresponding to the cDNA sequence set forth in SEQ. ID. NO. 1. Determination of expression products of this gene is proposed as having utility in predicting responsiveness to treatment with interferon-α and other interferons which act at the Type 1 interferon receptor. Therapeutic use of the protein encoded by the same gene is also envisaged.
CN103169724A Preparation method and application of oleanolic acid trisaccharide saponin component The invention relates to a preparation method of an oleanolic acid trisaccharide saponin component 3-O-beta-D-glucopyranose-(1 arrow 3)-alpha-L-rhamnopyranose-(1 arrow 2)-alpha-L-arabinopyranose oleanolic acid saponin and application of the component for resisting tumors. The invention also relates to application of an extract which is from rhizomes of Pulsatillachinensis(Bunge)Regel and contains the compound for resisting the tumors. The tumors include lung cancer, liver cancer, gastric cancer, colon cancer, glioma, breast cancer, cervical cancer, leukemia, lymph cancer and the like.
EP2185517A1 Process for preparing a leukotriene antagonist and an intermediate thereof Dicyclohexylamine salt of formula (IIa) or a pharmaceutically acceptable solvate thereof, including a hydrate, and its process for preparation. Process for the preparation of montelukast of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, including a hydrate, comprising the conversion of a salt of formula (IIa) into its form of free acid, followed by reaction with a compound of formula (III) CH3MgX, wherein X is halogen, in a suitable solvent, optionally in the presence of a Lewis acid.
EP2079690B1 3-aza-bicyclo[3.1.0]hexane derivatives The invention relates to 3-aza-bicyclo[3.1.0]hexane derivatives of formula (I) wherein A, B, n, X, and R1 are as described in the description, and salts thereof, and their use as orexin receptor antagonists.
US7241814 Preparation of metallic nanoparticles with shell-crosslinked micelle as mold A method for the preparation of a dispersion of fine particles characterized in that the micelles are ones which have been formed in a aqueous medium with an amphiphilic block copolymer represented by the general formula PB and in which the shell of each micelle has been cross-linked with hydrophilic groups of the hydrophilic side chains wherein the particles formed are metallic particles having a reducing characteristic of metal ions. The general formula PB is:
US7098203 and selective serotonin reuptake inhibitors; 4-benzyloxymethyl-4-phenylazepanes; antidepressants; anxiety The present disclosure relates to chemical compounds and their use in human therapy. In a specific embodiment, compounds of Formula (I) or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.
CN1784991A Method for preparing sour soymilk contg. micron Yinlanzha konjak sugar for reducing-weight and lowering blood-fat A micron-class health-care sour bean milk for decreasing fat and losing weight is prepared from traditional bean milk, micron-particles of gingko leaf, gynostemma penta phyllum, haw and konjak, chitosan, isomaltose ketone and useful intestinal bacteria through proportional mixing, processing and fermenting. Its advantages are high effect and rich nutrients including vitamins, minerals, etc.
US20100010074 Inhibiting Serum Response Factor (SRF) to Improve Glycemic Control Described are methods of improving glycemic control/improving insulin sensitivity by administering an inhibitor of serum response factor (SRF) activity, and methods of identifying new compounds for use in the described methods of treatment.
WO2009112541A3 Combination therapy with pm00104 and another antitumor agent [2-(6-fluoro-1H-indol-3-ylsulfanyl)benzyl]methyl amine and pharmaceutically acceptable salts thereof is provided for the treatment of CNS disorders, like mania, depression, bipolar disorder, anxiety, dementia, compulsive attention spectrum disorder, autism, impulse control disorder, conduct disorder, insomnia etc.
CN1981753A Medicine for controlling urine citric acid concentration and preventing nephrolithiasis A medicine for controlling the content of citric acid in urine and preventing and treating renal calculus is prepared from lithium citrate.
US20130045934 Extraction method using ultra fine bubbles and liquid extracts obtained thereof The present invention provides an extraction method that either does not use emulsifiers, organic solvents, and the like or can reduce the amount used of emulsifiers, organic solvents, and the like. In addition, the extraction method of present invention can also efficiently extract various components from various materials to be extracted, and can highly maintain potency and the like of the extracted components, in particular if the components are active agents. Furthermore, the extraction method of present invention has excellent safety. The extraction method of present invention is achieved by bringing materials to be extracted into contact with liquid containing ultra fine bubbles for extraction treatment. The ultra fine bubbles utilized during the extraction process preferably have a mode diameter of 500 nm or smaller and a concentration of 1,000,000 or more per 1 ml of liquid.
CN103505429A Gliguidone tablet The invention relates to a gliguidone tablet and a preparation method thereof, belonging to the field of medicine technology. The gliguidone tablet is characterized by consisting of gliguidone, lactose, microcrystalline cellulose, crosslinked sodium carboxymethylcellulose and magnesium stearate.
US20100173866 Apparatus and method for ocular treatment The invention provides tools, materials and related methods to surgically access the suprachoroidal space of an eye for the purpose of performing minimally invasive surgery or to deliver drugs to the eye. The invention provides a flexible microcannula or microcatheter device (11, 13) that may be placed into the suprachoroidal space (12, 14) through a small incision (12A) of the overlying tissues, maneuvered into the appropriate region of the space, and then activated to treat tissues adjacent to the distal tip of the device.
EP1660063A1 Use of bicyclo [2.2.1] heptane derivatives for the preparation of neuroprotective pharmaceutical compositions The invention relates to the use of compounds of the general Formula (I), wherein R3 stands for hydrogen or hydroxy; R1 stands for hydrogen or alkyl; and R2 stands for alkyl) and pharmaceutically acceptable acid addition salts for the preparation of pharmaceutical compositions having neuroprotective effect.
US20080009510 Fused Aminopiperidine as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes The present invention is directed to novel substituted fused aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
US20110003864 Crystalline 1-(3-fluorophenyl)-5-methyl-2-(1h)pyridone, the preparation methods, compositions and applications thereof Crystalline pyridone compound, which is the white needle crystal containing no water and other crystallization solvents. Its unit cell belongs to monoclinic system and has space group of P21/n, wherein a=3.8512(2), b=20.2535(12), c=12.1628(6) Å, β=92.850(5)° and crystal cell volume V=947.53(9) Å3. Pyridone compound crystal of this form has the needed properties for preparing or making treatment compositions in large scale. It can be used for treating organs fibrosis of liver, kidney, lung and etc. and reducing skin scars.
CN103520635A Compound zedoary oil expandable vaginal suppository, and preparation method and detection method thereof The invention relates to a compound zedoary oil expandable vaginal suppository, and a preparation method and a detection method thereof. The expandable vaginal suppository comprises active ingredients, a matrix and an expansion carrier. The active ingredients include an imidazole antimicrobial drug and zedoary oil; the drug-containing matrix of the expandable vaginal suppository contains povidone to increase solubility and stability of the zedoary oil; and the menthol can promote the absorption of the active ingredients. The compound zedoary oil expandable vaginal suppository is a hollow double-layer expandable suppository, and the suppository separates the matrix and the active components to further improve the stability of the active ingredients and prevent volatilization of zedoary oil, so as to improve the curative effect of the suppository. The compound zedoary oil expandable vaginal suppository employs six originally created leading technologies and has beneficial effects of prevention of liquid outflow, high stability and significant curative effect.
US7148212 Subjecting a supersaturated solution containing a steroid to wet milling while crystallizing, in order to obtain a primary particle suspension. The process for making steroid crystals having a predetermined average particle size of from 1 μm to 25 μm and a maximum particle size that does not exceed a predetermined maximum value of 100 μm, includes subjecting a supersaturated solution containing a steroid to a wet milling by wet milling apparatus while crystallizing, in order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described.
US20110118347 TREATMENT Of RINGWORM A compound of the formula CH3(CH2)n—RA—(CH2)m-(CH═CH)q—(CH2)p—X wherein RA=(a); q=0 or 1; m and p are independently selected integers of at least 1; n=0 or an integer of at least 1; X is a polar group selected from —CO2RS, where Rs═H, Na, K, —NHRI, —NRIRII or RIII; —CH3OH; —CH3NH2; —CH3NHRI; or —CH3NRIRII; wherein RI, RII and RIII are independently selected from C1-C6 alkyl or an aryl group, preferably a hydrophilically substituted C1-C6 alkyl or aryl group, or RIII is an esterified glycol; and wherein 20>m+n+p+2q≧2; is useful for the treatment of ringworm infection caused by Trichophyton tonsurans.
US20050096356 2-[[6-Methoxy-3-pyridinyl]methyl]amino-N-[3-(trifluoromethyl)phenyl]benzamide hydrochloride salt or its tautomer; treating retinopathy or age-related macula degeneration The invention relates to anthranilic acid amide derivatives of formula (I), wherein R1 represents H or lower alkyl, R2 represents H or lower alkyl, R3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age—related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.
CN101766617A Compound composition of intal and Statins The invention relates to a compound composition containing intal and statins claritin. The compound composition consists of the following components: a) a certain amount of intal; b) a certain amount of one of olopatadine hydrochloride, ioratadine, desloratadine, degreasing ioratadine, desloratadine, rupatadine and betahistine; c) other medicinal excipients. The compound composition can be made into external preparations such as eye drops, nose drops, aerosol, spray, inhalant, gelata, eye ointments, ointments or patch and the like. The compound composition can be used for curing the diseases such as anaphylactic eye diseases, anaphylactic rhinitis, skin urtication, urticaria, allergic asthma and the like, can significantly improve allergic symptoms, and has the characteristics of high efficiency, stability, safety, low adverse reaction rate, convenient use and the like.
WO2005013691A1 Use of boranocarbonates for the therapeutic delivery of carbon monoxide Boranocarbonates are described for administration to a human or other mammal for delivery of carbon monoxide. The boranocarbonate is a compound or ion adapted to make CO available for physiological effect, and may be administered with a guanylate cyclase stimulant or stabilizer. The physiological effect may be stimulation of neurotransmission, vasodilation or smooth muscle relaxation.
US20090004269 Pharmaceutical Composition Comprising a Proton Pump Inhibitor and a Protein Component The present disclosure relates to, inter alia, pharmaceutical compositions comprising a H+K+-ATPase proton pump inhibitor and a protein component; to methods for manufacture of such compositions, and to use of such compositions in treating and preventing diseases and/or disorders.
WO2006062982A3 Urea inhibitors of map kinases The present invention is directed to a compound having the formula (I) wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP Kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.
WO2006090250A1 Substituted 1,1,1-trifluoro-3-[(benzyl)-(pyrimidin-2-yl)-amino]-prop an-2-ol compounds Substituted 1,1,1-trifluoro-3-[(benzyl)-(pyrimidin-2-yl)-amino]-propan-2-ol compounds, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
CN101199647A Medicament compound agent for treating II model diabetes and reversing insulin resistive and preparing method thereof The invention aims at providing a compound medical preparation for clinically curing type II diabetes mellitus and reversing insulin resistance. The compound medical preparation contains effective ingredients and medical auxiliary materials, which are the mixture of epigallocatechin-3-gallate, any kind of tea polyphenol and cyclocarya paliurus (Batal.) iljinsk water extracts. The invention also provides a method to prepare the compound medical preparation. The compound medical preparation of the invention can be effectively used to clinically cure type II diabetes mellitus and reverse insulin resistance.
US8703208 Nanometer mesoporous silica-based xerogel styptic process and its preparing process and application The invention disclosed a novel mesoporous silica-based xerogel and its use in hemorrhage control. The mesoporous silica-based xerogel material has tunable mesopores (1-50 nm), high specific surface area (100-1400 m2/g), macroscopical morphology (powder, film, disc, column, etc.) and adjustable compositions (SiO2, CaO and P2O5, etc.) as well as good biodegradation. The mesoporous silica-based xerogels herein effectively promote the blood clotting under various conditions including slow and severe hemorrhage, even at the blood oozing site of bone defect. Meanwhile, the networks of silica-based xerogel with good elastic and mechanic properties, formed by adsorbing a large amount of water, can modulate the cell behavior and tissue growth, and thus promote the wound healing. Additionally, due to the mesoporous structure, the materials have the potential to load drug, thrombin and bioactive factors, which is favorable for the therapeutical efficacy.
CN101897716B Application of astilbin in preparing drugs capable of curing or preventing acute renal failure The invention provides an application of astilbin in preparing drugs capable of curing or preventing acute renal failure and kidney fibrosis.
CA2703125C Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer The present invention relates to pyrazine substituted pyrrolopyridines which are inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. Such compounds may be represented for example, by Formula II: (see formula II).
US20100305103 Genes differentially expressed in bipolar disorder and/or schizophrenia This invention provides molecular markers that are prognostic and/or diagnostic for a psychiatric disorder. In particular, genes are identified whose expression is altered in schizophrenia and/or bipolar disorder thereby providing prognostic and diagnostic markers for the disorder. In addition genes are identified whose dysregulation provides markers that allow diagnostic distinction between schizophrenia and bipolar disorder.
US20060281733 4-Bromo-5-(2-chloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide; 5-(2-chlorobenzoylamino)-1H-pyrazole-3-carboxylic acid {2-[4-(4,5-dihydro-1H-imidazol-2-yl)-phenyl]ethyl}amide; useful for the moderation of pain, septic shock, and scarring Disclosed are compounds of formula I and II that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.
CN103349717A Compound medicine for treating difficult-to-heal wounds, multiple wounds and suppurative diseases The invention provides compound medicine for treating difficult-to-heal wounds, multiple wounds and suppurative diseases. The medicine mainly comprises ascorbic acid, riboflavin, resina draconis, jaggery, erythrocin, pseudo-ginseng and borneol, and is prepared into medicine powder, an unguent and liquid medicine by adopting the method, wherein the medicine powder is mainly used for treating the multiple wounds such as a knife wound, a scald, a lacerated wound, an explosive wound, nipple rupture, crush wounds on hands and feet, and a wound that wood, bamboo and iron nails pierce into muscles and bones, and the suppurative diseases such as an abscess, an ulcer, phlegmon and multiple furuncles, carbuncles and malignant boils; the unguent is mainly used for treating various traumatic injuries, pruritus cutanea and mosquito bite injuries, and can relieve pains caused by symptoms such as a lumbar pain, a cervical vertebra pain, scapulohumeral periarthritis and wrist and ankle pains effectively; and the liquid medicine is mainly used for disinfecting the multiple wounds such as the abscess, the ulcer and the knife wound and removing pollutants, and can accelerate wound healing effectively. The medicine can treat the disease symptoms uniformly, and is instant in effectiveness, short in treatment course and low in expense; an effective ratio is 100%; a curative ratio is 98%; and a healing effect is remarkable.
CN101037428A Purification of sesquiterpene lactones A in achillea alpine and anti-tumour cell proliferative activity thereof The invention provides a sesquiterpene lactone compound Achillinin A separated from the Achillea millefolium. The invention also relates to the preparing method of said composition and the application to inhibit the tumor cells.
WO2012173099A1 Endothelial-lipase-inhibiting amino derivative A compound represented by formula or a pharmacologically permitted salt thereof. (In formula, X represents =CR4- or =N-; Y represents -CR5= or -N=; Z represents =CR7- or =N-; R4 and R7 represent hydrogen, halogens, or the like; R5 and R6 represent hydrogen, heteroaryls, or the like; R1 and R2 represent hydrogen, halogens, or the like; and R3 represents -(CR8R9)m-NR10R11 (in which m represents an integer from 0 to 3 and R8, R9, R10, and R11 represent hydrogen, alkyls, or the like.))
CN102018683A Effervescent tablet containing piracetam The invention relates to an effervescent tablet containing piracetam, which comprises piracetam, citric acids, sodium bicarbonates, oligosaccharides or other edible sugars, and the weight ratio of the piracetam to the citric acid to the sodium bicarbonate to the oligosaccharide or other edible sugars is (10 to 20): 30: 7: 200. The effervescent tablet in the invention has the advantages that the piracetam used as a functional composition is prepared into the effervescent tablet, therefore, compared with other medicament forms, the piracetam-containing effervescent tablet has the advantages of good stability, easy absorption, good taste, and capability of being directly soaked in water for drinking without mixing, and is easy to keep and dissolve.
CN101669929A Preparation method and application of ibuprofen liquid preparation The invention discloses a preparation method and an application of ibuprofen liquid preparation. After a plenty of experiment researches, the researchers of the invention finally find a way to preparethe ibuprofen liquid preparation. The preparation method comprises the steps of making ibuprofen and arginine into a compound, combining with proper accessories and making into liquid preparation. Bymaking ibuprofen and arginine into a compound, the invention can solve the problem of the inferior water-solubility of the ibuprofen. Making the compound into liquid preparation brings convenience tothe patient who can not take orally. The invention has fast effect and obvious anti-inflammatory and analgesic effect.
CN102600116A Application of teprenone in resisting neurotoxicity caused by methamphetamine The invention discloses an application of teprenone in the preparation of drugs for preventing and/or treating neurotoxicity caused by methamphetamine, belonging to the technical field of medicines. The teprenone has the effect of resisting neurotoxicity caused by methamphetamine. A test result shows that the teprenone has the capabilities of protecting rat pheochromocytoma cells, namely PC12 cells to be free from cell apoptosis caused by methamphetamine and recovering the pro-caspase3 protein reduction caused by methamphetamine, and has the advantages of obvious treatment effect, high safety, low cost and suitability for practical popularization and application.
EP1652913A1 New strain of lactic acid bacterium and edible compositions, drugs and veterinary products containing it The use of the said strain is particularly effective in the prevention/treatment of hepatic steatosis (fatty liver) and in nonalcoholic hepatic steatosis.
US20110092571 Compositions and methods for sirna inhibition of icam-1 RNA interference using small interfering RNAs which are specific for the ICAM-1 gene inhibits expression of this gene. Diseases which involve ICAM-1-mediated cell adhesion, such as inflammatory and autoimmune diseases, diabetic retinopathy and other complications arising from type I diabetes, age related macular degeneration and many types of cancer, can be treated by administering the small interfering RNAs.
WO2010139180A1 Naphthalene carboxamide derivatives as inhibitors of protein kinase and histone deacetylase, preparation methods and uses thereof The naphthalene carboxamide derivatives, the preparation methods and the uses thereof. The structure is shown as the formula (I), wherein the definitions of R1, R2, R3, R4 and Z are the same to those described in the description. The compounds have the protein kinase inhibition activities and the histone deacetylase inhibition activities simultaneously, and can be used for treating diseases related to protein kinase activity abnormity or histone deacetylase activity abnormity, including inflammation, autoimmune diseases, cancer, nervous system diseases and neurodegenerative diseases, metabolic diseases, angiocardiopathy, hypersusceptibility, asthma, and diseases related to hormone.
US20090197946 Composition and method for treatment of inflamation and infections of the genitalia, contraceptive and the prophylaxis of sexually transmitted diseases A composition, employed topically for its microbicidal, spermatocidal activity upon application to the human genitalia and/or anorectal area, and the prophylaxis of sexually transmitted diseases, contraception, and the relief from symptoms of local inflamation and infection. The embodiment incorporates L-Ascorbic acid in a concentration of about 2% to about 25% wt/vol, within an acidic range or pH level of about 4.0 to 2.0 pH respectively, in an aqueous solution with a pharmaceutically acceptable liquid carrier. In alternative exemplary embodiments the composition is in a specified physical state and predetermined composition for the desired therapeutic effect. Additionally, the composition in alternative embodiment includes a synergistic antioxidant and further incorporates enhancing bioactive ingredients. The method for topical application of the composition includes douche, rinse, cream, gel, suppository, saturated tampon and externally saturated condom for treatment of the vagina; drops, spray, cleansing wipe, cream, gel and internally saturated condom for treatment of the penis; and cleansing wipe, gel, suppository and externally saturated condom for male genitalia and rectum.
WO2007116012A1 Use of a d- and l-fucose-derived c-glycoside compound as an agent for activating and regulating cutaneous immunity The present invention relates to the use of compounds of general formula (I) derived from D- and L-fucose: as agents for stimulating the immune system of the skin and/or as immunoregulators, and for preparing a composition containing a cosmetically or pharmaceutically acceptable medium, intended in particular to prevent and/or limit the appearance of cutaneous immune imbalances, in particular related to environmental stresses.
US7262215 N-carbacycle monosubstituted indolocarbazoles as protein kinase inhibitors This invention relates to N-carbacycle monosubstituted indolocarbazole compounds. Furthermore, this invention relates to medicaments comprising N-carbacycle monosubstituted indolocarbazoles compounds and the use of such compounds for treating non-insulin dependent diabetes mellitus, acute stroke and other neurotraumatic injuries, for treating diabetes mellitus, as a chemotherapeutic for the treatment of various malignant diseases, for treating diseases caused by malfunctioning of specific signaling pathways, and for treating neurodegenerative diseases such as for example Alzheimer's disease.
CN101897673A Method for preparing vitamin C tablet The invention discloses a method for preparing a vitamin C tablet. The method comprises the following steps of: a, weighting the following raw materials: vitamin C, microcrystalline cellulose, hyprolose and sodium carboxymethyl starch; b, weighting 3 to 10g of octadecanol, adding the octadecanol into 100 ml of 80 to 95 percent of ethanol solution, and stirring the mixture to dissolve so as to prepare inclusion liquor; c, screening the vitamin C with a 100-mesh screen, putting the vitamin C into a fluidized drying bed or a stirrer, spraying the inclusion liquor in a volume mass ratio of 0.1:1 under the state of stirring, drying the mixture, and controlling the temperature to be between 45 and 55 DEG C; and d, putting the dried vitamin C into the stirrer, spraying the inclusion liquor in a volume mass ratio of 0.05-0.1:1 under the state of stirring, drying the mixture, uniformly mixing the included vitamin C and the remaining raw materials, and tabletting the mixture. Compared with the conventional wet granulation process, the method can improve production efficiency by 3 to 5 times and saves energy resources.
CN100998577A Triclosan compounding lotion for external use and its preparing method An exterior-applied lotion or gel of triclosan for preventing and treating the infectious gynecologic inflammation is proportionally prepared from triclosan, pronopol, gel matrix and other additives including surfactant. Its preparing process is also disclosed.
US20100204327 Methods for making retinoids and uses thereof Described herein are methods for making retinoids. Also described herein are retinoids and methods of use thereof.
CN102670620A Cefradine-borneol composition The invention discloses a cefradine-borneol composition belonging to the technical field of the preparation of medicines. The cefradine-borneol composition comprises cefradine and borneol according to the mass ratio of 1:0.1 to 1:10, wherein the optimal mass proportion is 1:1. The composition can be prepared into various medicament forms, such as tablets, capsules, granules, slow release preparations and injections, by using a conventional medicine preparation method and auxiliary materials which are universal pharmaceutically. The composition has a very good inhibiting action to various medicine-resistant bacteria, and the minimal inhibitory concentration (MIC) value is lowered at an order of magnitude. Therefore, the phenomenon of medicine resistance of common antibiotics is greatly improved, and the application prospect is extensive.
EP1787648A1 Medicinal composition for percutaneous perospirone administration A pharmaceutical composition for transdermal administration comprising perospirone of the formula (1): or a pharmaceutically acceptable acid addition salt thereof, which can inhibit the generation of metabolites and continuously maintain the blood level of perospirone.
EP1809236A1 Inhalation powder formulations containing enantiomerically pure beta-agonists The invention relates to inhalation powder formulations containing enantiomerically pure beta-agonists of formula (1), wherein the radicals R1, R2, R3 and R4 are defined as in claims and descriptions and are optionally embodied in the form the pharmaceutically acceptable acid addition salts thereof and are optionally combined with a pharmaceutically acceptable accessory agent. A method for producing said formulations and the use thereof in the form of a drug, in particular as a drug for treating respiratory tract diseases are also disclosed.
CN101244260A Combined medicament for treating chronic hepatitis B The invention provides the use for effective dose of Entecavir and/or the salt and effective dose of thymosin Alpha 1 in preparing the combined drugs which are used to curing chronic hepatitis B; the invention also provides a drug combined preparation for curing chronic hepatitis B, which has a favorable therapeutic effect for the sufferer which has no effect by singly using Entecavir. Meanwhile, the invention has the advantages of reduced usage for Entecavir and/or the slat, delayed generation for drug-resistant bacteria on the premise of ensuring the increased therapeutic effect, which provides a new, safe, effective drug selection for clinic.
EP1748995B1 Arylsulfonyl benzodioxanes useful for modulation the 5-ht6 receptor, the 5-ht2areceptor or both Compounds of the formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein m, n, p, Ar, X, R1, R2, R3, R4, R5 and R6 are as defined herein as well as compositions comprising these compounds and uses of the subject compounds for the preparation of medicaments for treating psychoses, schizophrenia, manic depressions, neurological disorders, memory disorders, attention deficit disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, food uptake disorders, Huntington's disease and gastrointestinal tract.
WO2007092095A3 [4-(benzo [b] thi0phen-2-yl) pyrimidin-2yl] -amine derivatives as ikk-beta inhibitors for the treatment of cancer and inflammatory diseases. The present invention provides compounds of Formula I: useful in the treatment of cancer and inflammatory diseases.
CN102920719A Compound veterinary medicine preparation for treating avian enteritis type colibacillosis The invention belongs to a compound veterinary medicine preparation for treating avian enteritis type colibacillosis in veterinary medicine. The preparation consists of three main medicinal components and an adjuvant; three main medicinal components include 3.25%W/W of neomycin sulfate, 0.81%W/W of lactic acid TMP (Trimethoprim) and 10%W/W of glutamine; and the adjuvant includes 85.94%W/W of glucose. The veterinary medicine preparation is utilized to treat the avian enteritis type colibacillosis. A processing technology of the composition is as follows: respectively grinding, screening and accurately weighing the components according to the necessary ratio, mixing for 25 min, and performing semi-finished product quality control, split charging, packaging and finished product quality control to obtain the composition. An application method is as follows: drinking the water in 1% level of the composition, and a course of treatment lasts for 4 days. The compound veterinary medicine preparation provided by the invention is remarkable in efficacy of avian enteritis type colibacillosis, low in drug resistance, safe and low toxicity, thereby having good popularization and application value.
US20090281059 Coating for a medical device having an anti-thrombotic conjugate A conjugate between an anti-thrombotic agent and bioabsorbable polymer is provided. Also, a method is provided for applying a coating comprising an anti-thrombotic agent and bioabsorbable polymer conjugate to at least some of an implantable device to prevent or reduce formation of thrombosis on the surface of the device. A first or sub-layer of the coating is prepared by mixing polymeric material and a biologically active agent with a solvent, thereby forming a homogeneous solution. A second or outer layer comprises an anti-thrombotic heparin-bioabsorbable polymer conjugate. This coating may be applied over inner drug-containing layers using, for example, dip coating or spray coating processes. After drying, the anti-thrombotic heparin bioabsorbable polymer conjugate remains in the outer layer of coating, allowing agent from the inner layer to elute there through. Also, the outmost layer prevents thrombosis, and can modulate release kinetics of agent(s) contained within inner layer(s) of the coating.
WO2012050985A1 Inhibitors of late sv40 factor (lsf) as cancer chemotherapeutics The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formulas (I)-(XXVI) as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC.
EP2346856A1 2-[1h-benzimidazol-2(3h)-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3h)-ylidene]-2-(pyrimidin-2-yl)acetamides as kinase inhibitors 2-[1H-benzimidazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and their salts are kinase inhibitors, useful in the treatment of cancer. Formula I
US7786162 Agents useful for reducing amyloid precursor protein and treating dementia and methods of use thereof The present invention provides compounds and methods of administering compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease βAPP production.
CN102871994A Flurbiprofen acetaminophen ester cyclodextrin inclusion compound and preparation method thereof The invention discloses a flurbiprofen acetaminophen ester cyclodextrin inclusion compound and a preparation method thereof. Anti-inflammatory and analgesic prodrugs mainly comprise brand new compounds of flurbiprofen acetaminophen ester, and a cyclodextrin inclusion process is adopted and includes dissolving the flurbiprofen acetaminophen ester in an organic solvent, adding the organic solvent containing the flurbiprofen acetaminophen ester into cyclodextrin or water solution of derivatives of the cyclodextrin, stirring and drying to form the inclusion compound easily dissolved in water. The inclusion compound can be further prepared into oral tablets or capsules by being mixed with proper adjuvents. By the flurbiprofen acetaminophen ester cyclodextrin inclusion compound and the preparation method thereof, solubility and dissolving-out speed of drugs can be remarkably increased, the solubility of the processed drugs in water is increased by 10-100 times as compared with that of crude drugs, cumulative dissolving-out percentage of the drugs in dissolving-out media in 45 minutes is substantially increased, and thereby oral absorption ratio of hydrophobic drugs of the flurbiprofen acetaminophen ester is improved.
CN103127074A Application of Aphanamixoid A to ileocecum cancer treatment medicine The invention discloses application of Aphanamixoid A to preparation of human ileocecum cancer treatment medicine and belongs to the technical field of novel application of medicine. In-vitro MTT antineoplastic activity evaluation shows that the Aphanamixoid A has the significant effect of inhibiting human ileocecum cancer cell lines HCT-8 from growing. Therefore, the Aphanamixoid A can be used for preparing the ileocecum cancer resistance medicine and has good development and application prospects. The application of the Aphanamixoid A to preparation of the human ileocecum cancer treatment medicine is made public for the first time, the skeleton type is fully novel, and inhibitory activity on the human ileocecum cancer cells is surprisingly strong.
WO2013062181A1 Capsosiphon fulvescens glycoprotein extract having liver protection effect and composition containing same The present invention relates to a capsosiphon fulvescens glycoprotein extract having a preventative effect against liver disorder caused by acetaminophen or carbon tetrachloride, and a pharmaceutical composition and a composition for health foods, containing same as an active ingredient. The capsosiphon fulvescens glycoprotein extract, the pharmaceutical composition, and the composition for health foods have an excellent remedial effect of inhibiting liver damage or liver disorder caused by acetaminophen or carbon tetrachloride and protecting the liver, are industrially applicable, and are economically efficient.
CA2425849C Angiostatic steroids Angiostatic steroids for use in controlling neovascularization and ocular hypertension are disclosed. Pharmaceutical compositions of the angiostatic steroids and methods for their use in treating neovascularization and ocular hypertension, including controlling the ocular hypertension associated with primary open angle glaucoma, are disclosed. Tn addition, the combination of the compounds with glucocorticoids for the prevention of elevated intraocular pressure during the treatment of inflammation is disclosed.
US20080207516 Co-administration of a polysaccharide with a chemotherapeutic agent for the treatment of cancer Disclosed herein are compositions and methods for treating diseases such as cancer. The compositions comprise one or more polysaccharides in an admixture with one or more therapeutic agents. This admixture can be administered to a subject in need thereof using any known method of administration. The therapeutic agent, if administered alone, can cause undesirable side-effects in the subject. The polysaccharide component minimizes or eliminates these side effects. The compositions described herein effectuate an enhanced therapeutic effect along with reduced toxicity.
WO2008034041A3 Therapeutic combinations The present invention provides a combination of (a) an antipsychotic and (b) an alpha4/beta2 (α4β2)-neuronal nicotinic receptor agonist. The invention further relates to pharmaceutical compositions comprising said combination and to the use of the combination in therapy. The invention further relates to a kit comprising the combination and use of said kit in therapy.
US20090081122 Injectable superparamagnetic nanoparticles for treatment by hyperthermia and use for forming an hyperthermic implant The injectable formulation for treatment by hyperthermia comprises a liquid carrier and heat-generating superparamagnetic iron oxide nanoparticles having a mean diameter not greater than 20 nm. Said injectable formulation is able to form in-situ a hyperthermic solid or semi-solid implant upon contact with a body fluid or tissue. Said hyperthermic solid or semi-solid implant may be useful for treating a tumor or a degenerative disc disease by hyperthermia.
US20110054039 Use of alkyl sulfates or sulfonates against propionibacterium acnes An alkyl sulphate or sulphonate having a carbon chain length of 11 or greater, for use in the treatment of a condition which is caused by, transmitted by and/or exacerbated by propionibacterial activity, in particular acne.
CN102732474A Compound for inhibiting mycobacterium tuberculosis, screening method and uses thereof The present invention discloses a screening method of a compound for inhibiting mycobacterium tuberculosis. The method comprises the following steps: (1) establishing a screening model adopting tyrosine phosphatase as a target point: adopting genome DNA of tubercle bacillus H37 Rv as a template, adopting a PCR technology to clone tyrosine phosphatase gene, transforming host cells, culturing the transformant to obtain recombinant tyrosine phosphatase from the culture, carrying out enzyme activity analysis, and establishing the screening model adopting tyrosine phosphatase as the target point; and (2) adopting the screening model established in the step (1) to screen a compound providing inhibition activity for the tyrosine phosphatase. With the method of the present invention, the tyrosine phosphatase inhibitor with anti-mycobacterium tuberculosis effect can be rapidly and efficiently screened. In addition, the present invention further discloses a compound screened by using the screening method, and uses of the compound in preparations of drugs for treatments of diseases, wherein the inducement or one of the inducements of the diseases is the tyrosine phosphatase.
US20100048717 Cathepsin b inhibitors Compounds of formula (I): are found to be selective inhibitors of cathepsin B, and hence useful in treating a variety of pathological conditions.
CN102188705A Medicament composition containing bis cyclooctane derivatives The invention relates to a medicament composition, in particular relating to a medicament composition containing a bis cyclooctane derivative. The medicament composition provided by the inveniton comprises a bis cyclooctane derivative shown in an expression (I), and at least one carrier accepted by cardiovascular and cerebrovascular disease medicament or pharmaceutically acceptable; and the invention further relates to a medicine box containing the active matters. The composition or the medicine box is used for preventing, retarding progression or treating the following diseases or symptoms: diabetes mellitus II, diabetes mellitus complication, hyperglycemia, obesity, insulin resistance, hypertension, hypertension complication, dyslipidemia, coronary heart disease, angina pectoris, congestive heart failure, arrhythmia, cerebral apoplexy, atherosclerosis, cerebral infarction, ischemic disease, cerebrovascular disease, cardiovascular disease, coronary artery disease, sexual dysfunction, cognitive dysfunction, ventricular dysfunction, cardiac insufficiency, pulmonary vascular disease or renovascular disease, thus reducing the morbidity and/or mortality of the cardiovascular and cerebrovascular diseases, decreasing the adverse effect, and improving the compliance of a patient during administration.
WO2014151462A1 Novel breathing control modulating compounds, and methods of using same The present invention includes pyrimido[5,4-d]pyrimidines that are useful in the prevention and/or treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of preventing and/or treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of the invention.
WO2005002589A1 Improvement of the hatching ability of egg-laying animals The invention relates to the use of pharmacologically compatible phosphonic acid derivatives for improving the hatching ability of egg-laying animals, especially birds.
CN102018665B Strictosamide injection and preparation method thereof The invention discloses a strictosamide injection which is characterized in that the injection/100ml contains the following raw materials based on weight ratio: 10-250mg of strictosamide, 800-1000mg of sodium chloride or 4500-5500mg of glucose, 50-400mg of one of sodium sulfite, sodium bisulfite, vitamin C or sodium thiosulfate, and the balance of water for injection. The strictosamide injection takes the strictosamide as an effective ingredient and takes the sodium sulfite, the sodium bisulfite, the vitamin C or the sodium thiosulfate as an antioxidant, takes sodium chloride or the glucose as an isotonizing agent and takes the water for injection as the solvent of the effective ingredients. According to the strictosamide injection, the defects of slow adsorption, long time for taking effect and low bioavailability are overcome, thereby not only increasing the effective dosage for clinics, but also providing preferable service for patients. In addition, as the antioxidant is further selected, the stability for transfusion can be ensured, and the security assurance is provided for clinic pharmacy.
US20090148541 Compositions and methods for the treatment of seborrhea Methods and compositions are provided for treating dermatological diseases, disorders, and pathologies, including seborrheic dermatitis, in a subject in need thereof. In some embodiments, methods are provided for the treatment of a dermatological disease, disorder, or pathology comprising, topically administering to a subject in need of dermatological treatment a composition comprising a therapeutically effective amount of bupropion, lithium or lithium salicylate, or combinations thereof.
EP1867644A1 Heteroaryl-tetrahydropiperidyl compounds useful for treating or preventing pain A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a "Tetrahydropiperidyl Compound"); compositions comprising an effective amount of a Tetrahydropiperidyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Tetrahydropiperidyl Compound are disclosed herein.
CN101543555A Combined medicine for treating burn and scald The invention discloses a medicine for treating burn and scald, which is prepared from proper amount of prepared coptis root, black sanguisorba root, folium ilicis chinensis, beautyberry, angelica dahurica, plaster of pairs, borneol and benne oil. The medicine has obvious effect on treating burn and scald, particularly two-degree or three-degree severe burn and scald, ensures that the burn-scald skin can rapidly recover with no scar left after healing, is convenient to use, has no any side effect, but has the effective rate of 100 percent and the cure rate of 99 percent. The medicine is easy to prepare and is ideal for treating the burn and the scald.
CN101987095A Application of daphnetin to preparation of medicament for treating rheumatism, rheumatoid arthritis and sprain caused by falling The invention discloses gel for treating rheumatism, rheumatoid arthritis and sprain caused by falling. The gel comprises daphnetin serving as an active ingredient, and a gel matrix, a humectant, a preservative agent and the like, and is used for treating pains in veins and muscles of waist and leg joints caused by the rheumatism, the rheumatoid arthritis and the sprain caused by falling. The invention also discloses a preparation method for the medicament. The medicament has the advantages of long storage time, no stimulation to skin mucosa, no foreign body sensation, no greasy feeling, no pollution on clothes, simple preparation process, high stability, convenience of storage and carrying, high permeability, obvious curative effect and no toxic or side effect, can be directly applied to joints or other lesion sites, is safe and convenient to apply, and the like.
US20100105722 Substituted 4,5,6,7-tetrahydrothienopyridines as KCNQ2/3 Modulators Substituted tetrahydrothienopyridines corresponding to formula (1) in which A1 through A3 and R1 through R12 have defined meanings, pharmaceutical compositions comprising such compounds, a process for preparing such compounds and the use of such compounds in treatment or inhibition of conditions mediated by the KCNQ 2/3 K+ channel, e.g., pain.
US8288570 7-iodo tetracyclines and related methods 7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.
WO2013142346A1 Premature-termination-codons readthrough compounds Premature termination codons readthrough compounds of formula (lb), composition thereof, and methods of making and using the same are provided.
CN102688248A Use of bufadienolide compound in preparing medicines for treating oral mucosal malignant tumors The invention discloses a use of a bufadienolide compound in preparing medicines for treating oral mucosal malignant tumors. Anti-cancer experiments of human tongue squamous cancer cells are carried out in vitro through a bufadienolide extract and monomeric compounds, namely gamabufalin, arenobufagin, telocinobufagin, bufotaline, cinobufagin, desacetylcinobufotalin, heloniogenin, resibufogenin, and cinobufotalin, and experimental results show that the bufadienolide compound has strong inhibition effect on tongue squamous cancer cells and compared with the bufadienolide extract and eight monomeric compounds, namely gamabufalin, arenobufagin, telocinobufagin, bufotaline, desacetylcinobufotalin, heloniogenin, resibufogenin, and cinobufotalin, cinobufagin has a stronger anti-tumor cell activity. The bufadienolide compound provided by the invention has clear components, controllable quality, strong anti-tumor activity and little adverse reaction and is expected to be developed into a novel anti oral mucosal malignant tumor medicine.
CN102070588A Alpha-pyrone compounds, and preparation method and application thereof The invention relates to alpha-pyrone compounds, and a preparation method and application thereof. The alpha-pyrone compounds with novel structure are prepared by nocardiopsis dassonvillei HR10-5 extracted from sea samples. Tests prove that the compounds can be used as a candida albicans inhibitor.
CN101550177A Effective component of radix pulsatillae and preparation method thereof The invention relates to an effective component of radix pulsatillae as well as a preparation method and an application thereof. The preparation method of the effective component comprises the following steps: (1) a mixture of ethyl acetate and ethanol is used as a solvent to extract the radix pulsatillae; (2) an extracting solution is processed by chromatography through a chromatographic column to obtain an eluent; and (3) the eluent is eluted by prepared liquid chromatogram gradient and is collected for 24.0-28.0 minutes, 28.0-32.0 minutes, 32.0-36.0 minutes, 48.0-52.0 minutes, 52.0-56.2 minutes and 60.0-64.0 minutes to obtain the effective component by taking water and acetonitrile as mobile phases.
US20080292710 Liquid Dosage Forms Of Acid Labile Drugs Liquid formulations of acid-labile drugs are provided. The formulations generally comprise micro-granules comprising an acid-labile drug coated with an enteric coating and a liquid vehicle having a pH less than 6.0. The components of the formulation can separately provided in the form of kits. The formulations and kits may be used to treat patients suffering from disorders for which the acid labile drugs are indicated.
WO2014072261A1 Triazolo compounds The present invention relates to compounds of formula (I) and its use for the treatment of neurological disorders.
US20120289556 Methods for Treating Conditions Caused by Higher-Than-Normal Dopaminergic Activity In Basal Ganglia Treatment of humans suffering from conditions caused by higher-than-normal dopaminergic activity in basal ganglia includes administering the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.
WO2005066156A1 Selective kinase inhibitors A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C1-4 alkyl, O, S, SO2, CO or CS and X1, X2, X3 and X4 are optionally substituted by 9 specific substituents or one can be nitrogen. Compositions comprising a carrier and at least one compound of formula (I) are also provided. Further provided are methods of treating tyrosine kinase-associated disease states by administering a compound of formula (I) and methods of suppressing the immune system of a subject by administering a compound of formula (I).
WO2006103690A1 A novel process for preparation of substantially pure glimepiride The present invention discloses a novel process for purification of trans-4-methyl cyclohexylamine HC1 and 4-[2-(3-Ethyl-4-methyl-2-carbonyl pyrrolidine amido) ethyl] benzene sulfonamide used in the synthesis of 3-Ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(trans-4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide(I), popularly known as Glimepiride. The present invention also discloses a novel purification of Glimepiride Form I (I), having the undesired cis isomer below 0.15%. Glimepiride (I) is useful in the treatment of diabetes mellitus.
CN102485735A 6-fructosamine-4-arylamidoquinazoline derivative and purpose thereof The invention discloses a 6-fructosamine-4-arylamidoquinazoline derivative with the structural formula of formula I or a pharmaceutically acceptable salt thereof, and relates to a preparation method and a purpose of above compounds. According to the invention, fructose is connected to a 4-arylamidoquinazoline derivative, so the water solubility of the compounds and the selectivity of the compounds to tumor cells are improved.
CN1799551A Process for preparing glucose injection and glucose sodium chloride injection The invention provides a glucose and sodium chloride injection, which is prepared from glucose 50g (or 100g, 200g, 500g), sodium chloride 9g and balancing water for injection to 1000ml through mixing, inspecting, encapsulating, sterilizing, lamp checking and packaging.
US20120015875 Use Of Oxandrolone In The Treatment Of Burns And Other Wounds The subject invention provides a method of treating burn-induced weight loss in a burn patient which comprises administering a therapeutically effective amount of an oxandrolone to the patient. The invention also provides a method of treating a wound in a patient suffering from a wound which comprises administering a therapeutically effective amount of an oxandrolone to the patient. The subject invention further provides a method of treating burn-induced weight loss in a burn patient which comprises administering a therapeutically effective amount of an oxandrolone in conjunction with a protein supplement to the patient.
US7652022 N-(4-(4-(4-hydroxyphenylamino)-pyrimidin-6-yl)-oxyphenyl)-N'-(3-trifluoromethylphenyl)-urea; The invention relates to the use of diaryl urea derivatives in the treatment of protein kinase dependent diseases or for the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diaryl urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising diaryl urea derivatives for the treatment of said diseases, diaryl urea derivatives for use in the treatment of said diseases, novel diaryl urea derivatives, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.
US20090149406 Plasmid PXL3179 or NV1FGF A prokaryotic recombinant host cell comprising a heterologous replication initiation protein that activates a conditional origin of replication and an extrachromosomal DNA molecule comprising a heterologous therapeutic gene and a conditional origin of replication whose functionality in the prokaryotic recombinant host cell requires a replication initiating protein which is foreign to the host cell is described. The host cell may comprise a pir gene having at least one mutation, which may occur in the pir gene copy number control region, the pir gene leucine zipper-like motif, or the pir gene DNA binding region.
CN101199599B Powders medicament for treating paediatrics laxness The invention relates to a Chinese drugs preparation, namely a powder medicament for treating infantile diarrhea. The medicament is made by following materials by weight: 10g of cinnamon, 10g of semen euryales, 10g of Atractylodes, 10g of cumin, 10g of putchuck, and 20g of limonite. The invention has advantages of novel formula, low cost, easy preparation and remarkable effect.
CA2839956A1 Prostaglandin receptor ep2 antagonists, derivatives, compositions, and uses related thereto The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflamation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.
EP1289520B1 Pharmaceutical compositions for the treatment of depression comprising famotidine The invention relates to the human therapeutic application of famotidine or its therapeutically acceptable salts for the treatment of depression or symptoms suggesting depression, including somatic depression, unipolar depression, functional diseases of psychic origin, atypical depression, dysthymia, bipolar affective disorders, seasonal depression and persistent mood disorder. The invention also relates to such application of a pharmaceutical composition and its manufacturing.
WO2013020371A1 Pim kinase inhibitor, preparation method and use thereof in drug preparation Provided is a PIM kinase inhibitor - a compound with a structural formula as represented by general formula I. Also provided are the isomer, diastereoisomer, enantiomer, tautomer and salt of the compound as represented by general formula I; the E, J, Q, X, Y, Z and m in general formula I are as defined in claim 1. A PIM kinase biochemical activity test shows that the compound (1-96) of the present invention has an obvious PIM-1 kinase activity inhibition effect. When the compound concentration is three micromoles, the PIM-2 kinase activity inhibition rate is as high as 100%. Therefore, the PIM kinase inhibitor of the present invention can be used to prepare drugs for treating and preventing cancers, autoimmune diseases, allergic reaction diseases, or organ transplant rejection, thus having better clinical application value. Also provided is a preparation method.
CN102614195A Triterpenoid composition of antrodia cinnamomea, preparation and analysis method thereof Disclosed are the isolation, purification and analysis of the triterpenoid compositions (including ergostane and lanostane) in the fruiting body of Antrodia cinnamomea using HPLC and NMR, as well as the stereo structures and the amounts of the triterpenoid compositions. The cytotoxicity of triterpenoids is also revealed. Based on the aforementioned techniques, the presence and amounts of ergostane and lanostane in the drugs, healthcare food or other goods are able to be detected.
CN101062119A Buccal tablets having function of preventing decayed tooth and the preparing method thereof The invention relates to a buccal tablet for treating caries and process for preparation, wherein the tablet is prepared from green tea polyphenols, giant knotweed rhizome powder, honeysuckle flower powder, vitamin C, soybean lecithin powder, xylitol, beta-cyclodextrin, starch gum, miropowdered silica gel and edible flavoring essence through steps of dressing, mixing and pelleting.
US8372431 Pharmaceutical composition comprising licarbazepine acetate A pharmaceutical composition comprising licarbazepine acetate, especially eslicarbazepine acetate, in combination with suitable excipients, in particular a binder, and a disintegrant. Also disclosed is a granulation process, especially a wet granulation process, for making the pharmaceutical composition.
WO2010007944A1 Nitrogenated bicyclic heterocyclic compound Disclosed is a nitrogenated bicyclic heterocyclic compound represented by general formula (1). The compound or a salt thereof exhibits a potent antagonistic activity on an EP1 receptor when administered to a human body or an animal. Therefore, the compound or a salt thereof is useful, for example, as an active ingredient for a pharmaceutical agent for preventing and/or treating overactive bladder. The compound or a salt thereof is also useful as an active ingredient for a pharmaceutical agent for preventing and/or treating a symptom such as frequent urination, urgency of urination or urinary incontinence.
US20080287455 Sulfanyl substituted phenyl methanones The present invention relates to compounds of formula I wherein R1, R2, R3, X, X1, and n are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. These compounds are good inhibitors of the glycine transporter 1 (GlyT-1) for the treatment CNS disorders, such as schizophrenia, cognitive impairment, and Alzheimer's disease.
WO2011150198A1 Azolyl urea compounds and methods of use thereof Provided herein are azolyl urea compounds for treatment of CSF-1R kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
EP2569298A1 Novel ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.
US20100215713 Scaffolds for follicle transplantation The present invention provides for a device comprising a scaffold composition, a bioactive composition and a bio-in-hibiting composition, wherein said bioactive and bio-inhibiting compositions are incorporated into or coated onto said scaffold composition, wherein said scaffold composition temporally supports survival and growth of resident follicles, migration and multiplication of stroma cells and spreading and organization of endothelial cells and new vessels wherein said bioactive composition regulates development of a resident follicle, formation of new blood vessels and chemoattraction and proliferation of stroma cells and wherein the bio-inhibiting composition regulates inhibition of the development of a second resident follicle. The presence of the bio-inhibiting composition within the scaffold is involved in the quiescence of the follicles in the primordial stage, which is important to restore fertility.
US20110280825 Extracorporeal devices and methods of treating complications of pregnancy The invention features extracorporeal methods for the treatment of a subject having a pregnancy related hypertensive disorder, such as pre-eclampsia or eclampsia. The invention also features devices used for the extracorporeal treatment of subjects have a pregnancy related hypertensive disorder, such as pre-eclampsia or eclampsia.
CN101926772A Polysaccharide nucleic acid fraction of bacillus calmette guerin lipid composition for livestock and freeze-dry preparation thereof The invention belongs to the field of animal drugs, and discloses a polysaccharide nucleic acid fraction of bacillus calmette guerin (BCG-PSN) lipid composition for livestock and a freeze-dry preparation thereof. The lipid composition comprises the following raw materials in parts by weight: 1 part of BCG-PSN, 10-55 parts of phospholipid, 1-10 parts of cholesterol and 0-5 parts of poloxamer 188. The lipid composition prepared by the invention has the advantages of high safety, high stability, favorable encapsulation rate and higher curative effect. The method of the invention is suitable for industrial mass production.
CN101669902A Polyene phosphatidyl choline injection and preparation method thereof The invention relates to a polyene phosphatidyl choline injection and a preparation method thereof. The prescriptive technique is stable and feasible, and the safety and stability of the product are good.
CN103626713A Aza (oxa)-cyclopentane-2- ketone (thione) compounds, medicine compositions thereof, preparation method and applications The invention belongs to the field of pharmacology, and relates to aza (oxa)-cyclopentane-2- ketone (thione) compounds shown in the formula I, medicine compositions thereof, a preparation method, applications in preparation of medicines treating diabetes and glucolipid metabolism, and especially applications in preparation of medicines treating II-type diabetes.
EP1770093A1 Pyrido¬2,3-d|pyrimidine derivatives as phosphodiesterase inhibitors The present invention relates to optionally substituted pyrido-[2,3-d]-pyrimidine-2,4(1H,3H)-diones or optionally substituted pyrido-[2,3-d]-pyrimidine-2(1H,3H)-ones, particularly to 1-(optionally substituted) phenyl-3-(optionally substituted heteroarylalkyl or arylalkyl)-pyrido-[2,3-d]pyrimidine-2,4(1H,3H)-diones and pyrido-[2,3-d]-pyrimidine-2(1H,3H)-ones, useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft rejection agents, anti-graft-vs-host disease agents, anti-allergic agents (e.g., asthma, rhinitis and atopic dermatitis), anti-autoimmune agents or analgetic agents, to their precursors, to their preparation and to pharmaceutical compositions using the compounds of the invention.
US20070287753 Intranasal Administration of Ketamine to Treat Depression Methods and compositions for the treatment of treatment-resistant depression are described. More specifically, the invention demonstrates that intranasal administration of ketamine is effective to ameliorate the symptoms of depression in a patient who has not responded to an adequate trial of one antidepressant in the current episode and has recurrent or chronic depressive symptoms (>2 years).
US20100119613 Process to activate extracts derived from living organisms using long wave uv irradiation and compositions comprising said activated extract The present invention relates to a method for producing an extract which is capable of inducing an antioxidant stress response comprising the step of treating an extract from organic material with UV light, said extract being derived from a non-mammalian cell or a non-mammalian organism and said cell or organism being capable of synthesizing polyunsaturated fatty acids. Furthermore, an extract capable of inducing an antioxidant stress response produced in accordance with the inventive methods, in particular an extract capable of inducing an antioxidant stress response for the preparation of a cosmetic composition is disclosed. The present invention also relates to a cosmetic composition comprising the inventive extract obtainable by the method provided herein.
WO2006054370A1 Gluconeogenesis inhibiting agent The present invention provides a gluconeogenesis inhibiting agent containing as an active ingredient corosolic acid, an analogous compound of corosolic acid, or a pharmaceutically acceptable salt thereof.
US7384646 Antiseptic disinfectant, and cosmetics and toiletries, medicine or food containing the same The purpose of the present invention is to provide antiseptic disinfectant, and cosmetics and toiletries, medicine or food containing the same, which enhance the antibacterial activity that 1,2-alkanediol originally have against a broad range of strains by compounding 1,2-alkanediol with 5-10 carbons and a certain fragrance component. The present invention relates to an antiseptic disinfectant, and cosmetics and toiletries, medicine or food containing the same, which include 1,2-alkanediol with 5-10 carbons, and one or more materials selected from a group of citral, geraniol, nerol, perillaldehyde, α-terpineol, dodecanol and L-carvone.
US20090082291 administering to a surgery patient in whom p53 protein is elevated as a result of a stress, a modified double stranded siRNA to down-regulate p53 in the patient The invention relates to a double-stranded compound, preferably an oligoribonucleotide, which down-regulates the expression of a human p53 gene. The invention also relates to a pharmaceutical composition comprising the compound, or a vector capable of expressing the oligoribonucleotide compound, and a pharmaceutically acceptable carrier. The present invention also contemplates a method of treating a patient suffering from alopecia or acute renal failure or other diseases comprising administering to the patient the pharmaceutical composition in a therapeutically effective dose so as to thereby treat the patient. The alopecia may be induced by chemotherapy or radiotherapy, and the patient may be suffering from cancer, in particular breast cancer.
WO2007006566A1 Pyridazine compounds as glycogen synthase kinase 3 inhibitors Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula (I) indicates a single bond or a double bond; X is O, S or N-R5; R1, R2 are independently selected from the group consisting of H, NH2, NH-C1-C6-alkyl, OH, =O, (i.e. a carbonyl group), C1-C6-alkoxy, halogen, methyl, C2-C4-alkyl, C3- C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-alkenyl, formyl, C1-C3-alkylcarbonyl, and an aromatic radical Ar, R1 and R2 together with the carbon atoms, to which they are attached, form a fused, saturated or unsaturated 5-, 6- or 7-membered C-bound carbocyclic or heterocyclic ring comprising 1 heteroatom, selected from nitrogen, oxygen and sulfur as ring member and O, 1 or 2 further heteroatoms, independently selected from O, S and N, as ring members, wherein the fused ring is unsubstituted or may carry 1 , 2 or 3 substituents selected, independently of each other, from the group of radicals R4 as defined below; R3 is hydrogen OH, halogen, CN, nitro, C1-C6-alkyl, fluorinated C1-C6-alkyl, C1-C6- hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, fluorinated C3-C7-cycloalkyl, C1-C6-alkoxy, C1-C6- hydroxyalkoxy, C1C6-alkoxy-C1-C6-alkoxy, fluorinated C1-C6-alkoxy, C1-C6- alkylthio, fluorinated-C1-C6 alkylthio, C1C6-alkylsulfinyl, fluorinated C1-C6- alkylsulfinyl, C1-C6-alkylsulfonyl, fluorinated C1-C6 alkylsulfonyl, C1C6- alkylcarbonyl, fluorinated C1C6-alkylcarbonyl, C1-C6-alkylcarbonylamino, fluorinated C1-C6-alkylcarbonylamino, carboxy, C1-C6-alkyloxycarbonyl, fluorinated C1-C6-alkoxycarbonyl, NRaRb, C(O)-NReRf, NH-C(O)-N ReRf, NRaRb-C1-C6-alkylene, O-NRaRb, etc. and wherein R4 and R5 are as defined in the specification and the claims.
EP1513510A1 The use of milnacipran for the treatment of tension-type headache The invention relates to the use of minlacipran, a serotonin and norepinephrine reuptake (SNRI), for the treatment of tension-type headache.
US20110177100 Targeting pax2 for the induction of defb1-mediated tumor immunity and cancer therapy Provided is a method of treating cancer in a subject by inhibiting expression of PAX2. An example of a cancer treated by the present method is prostate cancer. In the cancer treatment methods disclosed, the method of inhibiting expression of PAX2 can be by administration of a nucleic acid encoding an siRNA for PAX2. A method of treating cancer in a subject by administering DEFB1 is also provided. Similarly, provided is a method of treating cancer in a subject by increasing expression of DEFB1 in the subject.
US20100062993 Adenosine Nucleotides as Dietary Supplements and as Agents in the Prevention of Cancer and the Metastasis Thereof It is the embodiment of this invention that Methylthioadenosine and its pharmaceutically acceptable salts as dietary supplements are more efficient, more economical and better tolerated than conventional existing dietary supplements such as S-Adenosylmethionine in the promotion of normal cell growth. It is a further embodiment of this invention that Methylthioadenosine and its pharmaceutically acceptable salts as dietary supplements are more efficient, more economical and better tolerated than conventional existing dietary supplements such as S-Adenosylmethionine in the destruction of aberrant cells that can cause various cancer. It is a further embodiment of this invention that Methylthioadenosine and its pharmaceutically acceptable salts as dietary supplements are more efficient, more economical and better tolerated than conventional existing dietary supplements such as S-Adenosylmethionine in the prevention of cancer cell metastasis
CA2405050C Production of tcr gamma delta t cells The method for obtaining and expanding TcR.gamma..delta.+ T cells in culture is described. The method involves: (1) culturing cells from a sample containing TcR.gamma..delta.+ T cells or precursors thereof in a first culture medium comprising a T cell mitogen and at least two growth factors and (2) culturing the cells obtained in step (1) in a second culture medium comprising at least two growth factors. The two growth factors are factors with interleukin-2-like and interleukin-7-like activity. The TcR.gamma..delta.+ T cells obtained by the method can be used in a variety of experimental, therapeutic and commercial applications.
WO2014036427A1 Biotin complexes for treatment and diagnosis of alzheimer's disease Described herein are compositions and methods for treating or imaging Alzheimer's disease (AD). The compositions comprise a biotin moiety and a siRNA moiety, without the need for a targeting agent such as an antibody, avidin, or streptavidin. In certain embodiments, the compositions further comprise a diagnostic agent.
CN101293101A Gamma-polyglutamic acid-vanadyl complexes, preparation and application thereof The invention relates to a Gamma-PGA-vanadyl complex, a preparation thereof and application, which pertains to the organic vanadium compounds and the technical field of the preparation and the application. The composite is formed by connecting the carboxyl group of the Gamma-PGA and the coordination bond on VOSO4 formed by VO<2 +>, and the molecular structural general formula is: (VO<2 +>) m-(Gamma-PGA), wherein, m is a positive integer ranging from 2500 to 6000. The commercial bacteria is utilized to carry out the fermentation, the separation and the purification of the Gamma-PGA, the Gamma-PGA and the VOSO4 are carried out the modification reaction, thus obtaining a crude product of the VO-Gamma-PGA composite, and the VO-Gamma-PGA composite is further obtained by centrifugalization and vacuum drying. The Gamma-PGA-vanadyl composite has the advantages that: the Gamma-PGA is taken as a carrier, the molecular weight thereof is large, thus playing the role of realizing the sustained release of the carrying drug, the biocompatibility is great, and the Gamma-PGA-vanadyl composite is non-toxic. The carrier Gamma-PGA is obtained by the microbial fermentation and preparation, the structure is homogeneous, the molecular weight is larger and the cost is low.
WO2006051399A1 Piperazine derivatives useful as adrenergic receptor antagonists The present invention relates to α1a and/or α1d adrenergic receptor antagonists, of formula I, which can be used to treat a disease or disorder mediated through α1a and/or α1dadrenergic receptors. Compounds and pharmaceutical compositions described herein can be used to treat benign prostatic hyperplasia (BPH) and related symptoms thereof. Further, such compounds can be used to treat lower urinary tract symptoms that may or may not be associated with BPH. The present invention also relates to processes to prepare the described compounds, pharmaceutical compositions thereof, and methods of treating BPH or related symptoms thereof.
CN101955493A Method for preparing cefotiam hexetil hydrochloride and composition of cefotiam hexetil hydrochloride The invention belongs to medicaments and in particular discloses a method for preparing cefotiam hexetil hydrochloride and a composition of the cefotiam hexetil hydrochloride. The method comprises the following steps that: the cefotiam hexetil is reacted with carbonate to obtain a cefotiam hexetil; the cefotiam hexetil is reacted with carbonic acid 1-iodoethyl ester cyclohexyl ester; and the reactant is extracted and frozen to obtain the cefotiam hexetil hydrochloride and composite tablets, capsules or particles and the like, which contain the cefotiam hexetil hydrochloride prepared by the method. The preparation method has the advantages of simple and convenient operation, capability of reducing environmental pollution, high purity and high yield of the obtained product.
EP1496888A1 Non-toxix amounts of protein-aggregating substances stimulate hsp70 expression and function as anti-tumor agents The present invention relates to the use of a drug inducing intracellular protein aggregation for the preparation of a pharmaceutical composition wherein the drug is in a dose of 135-175 mg/m2 body surface for the treatment of a tumor, a bacterial infection or a viral infection. Preferably said drug is selected from vincristine and paclitaxel. The present invention further relates to a method, of treating a patient suffering from a tumor, a bacterial infection or a viral infection comprising administering to said patient a drug inducing intracellular protein aggregation in a dose of 135-175 mg/m2 body surface. It is preferred that said drug is administered in combination with heat treatment.
WO2012157647A1 Method for selecting chemotherapy for gastric cancer patient using combination drug of tegafur, gimeracil and oteracil potassium and egfr inhibitor The present invention provides a method for predicting the therapeutic effect of a chemotherapy for a gastric caner patient using a combination drug of tegafur, gimeracil and oteracil potassium, said method comprising steps (1) to (3): (1) a step for measuring the expression amount of EGFR contained in a biosample collected from the patient; (2) a step for comparing the expression amount of EGFR determined in step (1) with a preset cutoff point corresponding thereto; and (3) a step for, on the basis of the results of the comparison in step (2), when the expression amount of EGFR is larger than the cutoff point, predicting that a sufficient therapeutic effect is likely to be achieved on the patient by selecting a chemotherapy using the combination drug of tegafur, gimeracil and oteracil potassium together with an EGFR inhibitor, or when the expression amount of EGFR is not larger than the cutoff point, predicting that a sufficient therapeutic effect is likely to be achieved on the patient by selecting a chemotherapy using the combination drug of tegafur, gimeracil and oteracil potassium alone.
US20060189558 Delivery of substances to cells Aggregates comprising VP22 protein and oligonucleotides or polynucleotides can be used together with a disaggregating agent (simultaneously or sequentially) to treat target cells by delivery of molecules to the cells and/or to prevent cell proliferation and/or to kill cells.
CN101538270A 8-alkyl galanthamine salt and preparation method and applications thereof The invention discloses 8-alkyl galanthamine salt which has a general formula as follows, wherein R is alkyl with 1-24 carbon atoms, and X<-> is fluorine, chloride, bromine or iodine ions; the invention also discloses a preparation method and applications of the 8-alkyl galanthamine salt; the 8-alkyl galanthamine salt is prepared by reflux reaction of galanthamine and alkylogen in solvent, with easy and feasible operation, high yield and low cost; and experimental results on in vitro inhibitory of activity of acetylcholinesterase show that compared with galanthamine salt, the 8-alkyl galanthamine salt has stronger inhibitory activity of acetylcholinesterase, and can be used in the preparation of high-efficiency and safe anti-Alzheimer's disease drugs, with good application prospect.
CN101381395A Pentacyclic triterpene saponins compounds, preparation method and use The invention discloses a pentacyclic triterpene saponin compound and a preparation method and application thereof. The compound has the following structure. Compared with Ardisia crispa saponin B, the compound has improved water solubility anticancer, activity equivalent to that of a substrate, milder reaction conditions, less pollution and lower cost.
CN101730690A Sulfonamide compound, and crystal thereof Disclosed are (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3- (methylamino)pyrrolidine monohydrochloride and a crystal thereof, each of which has excellent properties for use as an active ingredient of a pharmaceutical agent for the prevention and/or treatment of glaucoma or the like. The above-mentioned monohydrochloride crystal may have a main peak at at least one position selected from the group consisting of angle 2theta of about 13.9 DEG , 21.5 DEG , 21.7 DEG , 22.4 DEG , 22.8 DEG , 24.5 DEG and 35.0 DEG in powder x-ray diffraction spectra.
CN103251648A Iron-based montmorillonite medicine for treating hyperphosphatemia and iron-deficiency anemia and preparation method of iron-based montmorillonite medicine The invention relates to an iron-based montmorillonite medicine for treating hyperphosphatemia and iron-deficiency anemia and a preparation method thereof. The iron-based montmorillonite medicine contains an iron-based montmorillonite effective ingredient, wherein the iron-based montmorillonite (Fe-montmorillonite) is obtained by soaking or eluting medicinal montmorillonite with a water soluble iron salt solution. A preparation prepared by the effective ingredient of the iron-based montmorillonite medicine and adding with pharmaceutic adjuvant is administrated by virtue of a gastrointestinal tract, and the effective ingredient and phosphate in a digestive tract of a patient are combined into an insoluble substance and discharged from the body by virtue of the digestive tract, so that phosphate in the digestive tract of a patient suffering from chronic renal failure is reduced, and the aim of treating hyperphosphatemia is achieved; and the iron-based montmorillonite dissociates iron ions uncombined with phosphate, the iron ions umcombined with phosphate are absorbed by a human body, iron ions in the human body are supplemented, and the aim of treating iron-deficiency anemia of the patient suffering from the chronic renal failure is achieved, so that the iron-based montmorillonite medicine also can serve as a preventive used for preventing hyperphosphatemia and iron-deficiency anemia of the patient suffering from the chronic renal failure.
CN1850070A Quercetin solid liposome nano particle preparation and its preparing method The present invention relates to a quercetin solid lipid nano granule preparation and its preparation method, belonging to the field of medicine technology. Said invention uses quercetin as raw material medicine, adopts the mixture of solid lipid, emulsifier and emulsification adjuvant as medicine carrier and utilizes a certain preparation process so as to obtain the invented product. Said invention also provides the concrete steps of said preparation process.
EP2484358A1 Agent for inhibiting decrease of visceral fat in patient with parkinson's disease Provided is an inhibitor of visceral fat loss, which is capable of suppressing body weight loss peculiarly found in Parkinson's disease patients. The inhibitor of visceral fat loss in Parkinson's disease patients of the present invention contains a lipid obtained by subjecting a medium-chain triglyceride that includes as a constitutive fatty acid at least one of a saturated fatty acid having 8 carbon atoms and a saturated fatty acid having 10 carbon atoms to a transesterification reaction with a vegetable oil. The lipid is preferably obtained by subjecting the medium-chain triglyceride to a transesterification reaction with the vegetable oil at a ratio of 10:90 to 20:80.
US20060034837 Method and agents for the prevention, inhibition and therapy of cancers Disclosed are uses of Gangliosides GM1 and/or asialo-GM1 substances simulating the carbohydrate portion of said gangliosides with regard to bonding to anti-GM1 antibodies and/or anti-ADM1 antibodies for producing agents which bind or block anti-GM1 antibodies and/or anti-AGM1 antibodies which bond to natural killer cells (NKC) or for blocking antigen-presenting cells and producing a T-cell anergy, and for producing an affinity material for the extracorporeal removal of anti-GM1 antibodies and/or anti-AGM1 antibodies I order to prevent, inhibit, and treat malignant cancers.
CN101099738A Application of sanguinarine in preparing aquatic animal medicine and method for preparing its preparation The present invention discloses an application of sanguinarine in preparation of medicine for killing fish pathogenic bacteria and ectoparasite and preparation of its prophylactico-therapeutic preparation. Said prophylactico-therapeutic preparation is formed from sanguinarine, surfactant and solvent. Its preparation method includes the following steps: (1), making the sanguinarine be completely dissolved in a solvent with 40deg.C-50deg.C to obtain the solution containing 5%-20% of sanguinarine; and (2), making the surfactant and the solution obtained in step (1) be added into a homogenizing machine and uniformly mixed so as to obtain the invented product.
US6914063 Imidazo-pyrazine derivatives as ligands for GABA receptors A class of imidazo[1,2-α]pyrazine analogues substituted in the 3-position by a substituted phenyl ring, being selective ligands for GABAA receptors which interact more favourably with the α2 and/or α3 subunit than with the α1 subunit, are accordingly of benefit in the treatment and/or prevention of a variety of disorders of the central nervous system, including anxiety and convulsions, with a reduced propensity to cause sedation.
CN102327269A Solid lipidosome preparation of compound cefaclor medicinal composition The invention discloses a solid lipidosome preparation of a compound cefaclor medicinal composition and a preparation method thereof. A compound cefaclor medicinal composition lipidosome with excellent quality can be formed by selecting cefaclor, bromhexine, dimyristoylphosphatidylcholine, cholesterol and tween 20 in a specific weight proportion; and the lipidosome is prepared into the solid preparation by adopting a general preparation method. Compared with the prior art, the preparation disclosed by the invention has the advantages of greatly-improved quality of a preparation product, reduced toxic or side effects, high bioavailability, stable medicament release and more remarkable curative effect.
EP1307185B1 Use of carboanhydrase inhibitors for the prevention of diabetic retinopathy in diabetics Use of a carbonic anhydrase inhibitor in the preparation of a medicament for the prevention and treatment of diabetic retinopathy and various other retinopathies.
CN102973563A Application of ombination of esveratrol and piperine used for preparation of medicament for treatment of depression The present invention relates to a drug combination therapy. The combination of esveratrol and piperine are used for treating depression. Animal experiments show that the combination of esveratrol and piperine has a good anti-depressant effect, and is a relatively promising natural anti-depressant medicament, and can be used for the preparation of a medicament for the treatment of depression.
CN101993370A Glaucocalyxin A acid ester derivative as well as preparation method and application of Glaucocalyxin A acid ester derivative The invention discloses a structure of a Glaucocalyxin A acid ester derivative as well as a preparation method and an application of the Glaucocalyxin A acid ester derivative in treating cancers. The molecular structure of the Glaucocalyxin A acid ester derivative has a general formula as shown in the specification, wherein R1 and R2 are succinic acid substituent-C4H5O4, glutaric acid substituent-C5H7O4M, glycine derivative substituent-C6H8NO5 of succinic acid, and glycine substituent-C7H10NO5 or glycine substituent-OH of glutaric acid. The preparation method has the following steps: in the presence of tetrahydrofuran and 4-dimethylamino pyridine, the extracted Glaucocalyxin A and succinic acid or glutaric acid are reacted to obtain the succinic acid ester or glutaric acid ester of the Glaucocalyxin A disclosed in the invention, and the Glaucocalyxin A acid ester derivative reacts with N-Hydroxysuccinimide and glycine in turn in the presence of a buffer solution of tetrahydrofuran and phosphate to obtain the derivative of the acid ester of the Glaucocalyxin A and the glycine disclosed in the invention.
US20120094987 SUBSTITUTED PYRIDO [3', 2': 4, 5] THIENO [3, 2-D] PYRIMIDINES AND PYRIDO [3', 2': 4, 5] FURO [3, 2-D] PYRIMIDINES USED AS INHIBITORS OF THE PDE-4 AND/OR THE RELEASE OF TNF-alpha The invention relates to compounds of general formula (I); 1a, 1b, 1c and 1d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNFα-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.
US20100196462 Method for Manufacturing a Pharmaceutical Form of Oseltamivir Phosphate The invention relates to a method for manufacturing a pharmaceutical form of oseltamivir phosphate, characterized by including the following steps: a) compacting followed by calibration of an oseltamivir phosphate powder, b) dry mixing with the known product excipients obtained from the previous step, following by calibration. Application to industrial production adapted to a crisis situation such as a pandemic.
CN101932320A Membrane fusion inhibitor Disclosed is a preparation which is highly safe, which targets for a different stage in the virus growth cycle from a conventional one, and which can be used in an anti-viral agent. A preparation comprising an epigallocatechin gallate derivative represented by Chemical formula (1) or an isomer or salt thereof is prepared. The preparation can be used as a membrane fusion inhibitor which can inhibit the membrane fusion of a virus. In the formula shown below, R1 to R6 independently represent a hydrogen atom, a halogen, a sodium, a potassium, or a linear or branched saturated or unsaturated acyl group, provided that R1 to R6 may be the same as or different from one another, the acyl group may be further substituted by one or more substituents, and at least one of R1 to R6 represents the acyl group; and R7 to R16 independently represent a hydrogen atom, a halogen, a sodium or a potassium, and may be the same as or different from one another.
US20110262565 PIP-2 Inhibition-Based Antiviral and Anti-Hyperlipidemic Therapies Interaction of a specific viral domain with phosphatidylinositol 4,5-bisphosphate (PIP 2) is shown to mediate viral replication. Basic Amino Acid PIP-2 Pincer (BAAPP) domains are described herein, including, without limitation, NS5A protein of HCV, NS4B protein of HCV, poliovirus, and rhinovirus.
CN102246793A Antimicrobial composition and use thereof The invention aims to provide an antimicrobial composition which is simple in formula and low in cost. When the antimicrobial composition is used, the antimicrobial effect can be ensured by a small dose of antimicrobial ingredient. Another aim of the invention is to provide the new use of a chemical composition in the preparation of antimicrobial products. The invention discloses the use of the chemical composition consisting of ethanol, polyhexamethylene biguanidine (PHMB) or salt of the polyhexamethylene biguanidine and isopropanol in preparation of antimicrobial composition products. The total weight of the ethanol and the isopropanol is not less than 48 to 80 percent.
US20050037097 Pyruvate enriched onion extract Extracts of plants of the genus Allium, such as onion bulbs (Allium cepa), contain pyruvic acid and possess the ability to inhibit generation of organic free radicals, quench pre-formed free radicals, and to induce the activity of antioxidant enzymes such as quinone reductase, thus limiting damage due to aging such as cataracts.
CN101461790B Lamivudine tablet and preparation method The invention relates to a lamivudine tablet and a preparation method thereof, which solve the problem of expensive cost due to the fact that lamivudine is provided by foreign companies at present. The lamivudine tablet consists of the following raw materials by weight portion: 100 portions of lamivudine, 90 to 110 portions of microcrystalline cellulose, 15 to 25 portions of carboxymethyl starch sodium, 1 to 5 portions of hydroxypropyl methyl cellulose, 1 to 5 portions of magnesium stearate, and 90 to 110 portions of 50 percent alcohol. The lamivudine tablet has convenient raw material sources, low cost, simple production process, and convenient and quick operation, and is easy to process a main medicine, namely the lamivudine with an active ingredient into a tablet which satisfies the drug standard; and the preparation method has a simple and easy process, and steady and controllable product quality.
EP1855661B1 Formulation for aviptadil The present invention relates to pharmaceutical formulations of Aviptadil and its derivatives. The stability of the Aviptadil formulation was shown to be improved by a formulation having a defined concentration of Aviptadil prepared in a buffer having a defined pH range.
CN102614266A Drug for treating hypertension and hyperlipidemia The invention discloses a drug for treating hypertension and hyperlipidemia, which is mainly prepared from 1-1.5g of sanhuang tablets, 0.2-5g of analgin tablets and 0.3-0.6g of aspirin. The drug selects the sanhuang tablets, the analgin tablets and the aspirin to composite, the medicines are composited to generate a synergistic effect of all the medicine efficacies, and accordingly, the efficacies of effectively discharging fire, bringing down medium fever, dredging vessels and neutralizing hypertension viruses are obtained. Because the invention adopts the technical scheme, compared with the prior art, the drug has the advantages of obvious curative effect, no toxic side effect, stable long-term effect, convenience for oral taken and low price.
WO2014110344A1 Meglumine salt forms of 2-((1 r,4r)-4-(4-(5-(benzoxazol-2-ylamino)pyridin-2-yl)phenyl)cyclohexyl) acetic acid and their use as dgat1 inhibitors The present invention relates to novel crystalline forms of meglumine salts of 2-((1 R,4R)-4-(4-(5-(benzo[d]oxazol-2-ylamino)pyridin-2-yl) phenyl)cyclohexyl)acetic acid :Formule(I) and their use in the treatment or prevention of a condition or a disorder associated with DGATl activity in animals, particularly humans.
CN101204364A Delivery system and application of chitosan mucosa compromising mucosal adjuvant The invention relates to a chitosan mucosal delivery system, and the invention comprises two components which are the target antigen nanoparticles and the mucosal adjuvant nanoparticles. The target antigen nanoparticle comprises chitosan and target antigen coding plasmid DNA; the mucosal adjuvant nanoparticle comprises chitosan and mucosal adjuvant coding plasmid DNA. The mucosal vaccine which is produced according to the mucosal delivery system comprises two components, a component is the chitosan-VP1 nanoparticle which is formed by the chitosan and the plasmid of the coding CVB3 structural protein VP1 and the other component is the chitosan-VP1 nanoparticle which is formed by the chitosan and the plasmid of the coding lymphocyte chemotactic factor. By using the mucosal delivery system to carry out the mucosal immunity, the secreting of CVB3 specific generalization IgG and intestinal tract SIgA is induced effectively, and the occurrence of the Coxsackie vital myocarditis is effectively prevented.
CN101249080A Acetylkitasamycin dispersible tablet and method of preparing the same The invention relates to a novel acetylkitasamycin dispersible tablet and a preparation method thereof. The acetylkitasamycin dispersible tablet contains 20-60% of acetylkitasamycin by weight and 80-40% of pharmaceutically-acceptable adjuvant by weight including at least one selected from disintegrating agent, filling agent, lubricating binder and lubricant, wherein acetylkitasamycin contains acetylkitasamycin A6, acetylkitasamycin A7, acetylkitasamycin A4, acetylkitasamycin A5, acetylkitasamycin A1, acetylkitasamycin A3 and acetylkitasamycin A13 as major components. The preparation method of the acetylkitasamycin dispersible tablet involves wet-method granulation tableting process. The inventive acetylkitasamycin dispersible tablet has the advantages of rapid disintegration speed, convenient administration, less side effect, easy absorption, high bioavailability and blood drug concentration, and improved antibacterial effect. The preparation method is similar to the common tablet and is easy to be operate and control.
WO2006056479A1 Sly1 inhibitors in transplantation The present invention relates to a pharmaceutical composition comprising an inhibitor/negative regulator/antagonist of SLY-1 (SH3 domain protein expressed in lymphocytes). The use of an inhibitor/negative regulator/antagonist of SLY-1 for the preparation of a pharmaceutical composition for the treatment or prevention of undesired side effects in transplantation of cells, tissues or organs and/or for the treatment of graft-versus-host disease. Furthermore, a method is also described for treating or preventing undesired side effects in transplantation of cells, tissues or organs in a subject comprising administering an inhibitor/negative regulator/antagonist of SLY-1 to mammal in need of such a therapy is provided. The present invention also relates to a method for screening inhibitors or negative regulators of SLY-1 activity or expression comprising the steps of (a) contacting a cell or a non-human organism expressing SLY-1 or capable of expressing SLY-1 with a compound to be tested; (b) determining antigen-receptor signal transductions in the presence of said compound to be tested when compared to a cell not contacted with said compound; and (c) identifying the compound which inhibits SLY-1 activity.
US20110118243 Anti-inflammatory drug delivery system The invention provides dosage forms for the delivery of one or more non-steroidal anti-inflammatory drugs to equines. The dosage forms are palatable, desirable, and easy to administer with little or no mess or waste. The dosage form can be a cookie that includes one or more grain products, one or more protein products, one or more flavoring agents, or a combination thereof. The dosage form also includes a therapeutically effective amount of one or more non-steroidal anti-inflammatory drugs, for example, for the treatment of joint deterioration, swelling and inflammation, founder, fever, laminitis, or a combination thereof. The drug can be phenylbutazone or firocoxib and the dosage unit can be conveniently hand-fed to the horse.
US20100298405 Compositions And Methods For Inhibiting Expression Of Huntingtin Gene The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of the Huntingtin gene (HD gene), comprising an antisense strand having a nucleotide sequence which is less than 25 nucleotides in length and which is substantially complementary to at least a part of the HD gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of the HD gene, or a mutant form thereof, using the pharmaceutical composition; and methods for inhibiting the expression of the huntingtin gene in a cell.
WO2009114814A3 Therapeutic substances that modulate genome methylation Compounds containing nucleic acid bases or their precursors modified by enrichment at specific sites with heavy stable isotopes of elements naturally present at those sites in minute amount are useful for the treatment of diseases characterized by altered gene expression and altered pattern of epigenomic control. These compounds, when used as nutrients or in other medicinal application methods, can alter the DNA methylation pattern in a simple way through the well-understood mechanism of kinetic isotope effect (KIE). This effect could also be useful for modifying methylation kinetics in stem cell technology, cloning and as disease therapeutics.
CA2251840C Composition, barrier film, and method for preventing contact dermatitis The present invention relates to a composition, and a method for preventing or reducing contact dermatitis. The composition contains a polysaccharide; a low molecular weight, synergistic saccharide; a solvent; and optionally an additive material. The present invention is further a dermatologically-compatible barrier film for preventing and reducing contact dermatitis which contains a polysaccharide; a low molecular weight, synergistic saccharide; and optionally one or more additives. The dermatologically-compatible barrier film is formed of a composition containing a polysaccharide; a low molecular weight, synergistic saccharide; a solvent; and optionally an additive material.The composition is a skin care product in a form of a lotion, a gel or a cream that is applied to skin of mammals. Once applied, the solvent in the composition evaporates, and thereby leaves behind a dermatologically-compatible barrier film containing a polysaccharide; a low molecular weight, synergistic saccharide; and optionally an additive material.
CN102973601A Medicated bath film forming agent for preventing bouine mastitis and preparation method of medicated bath film forming agent The invention discloses a medicated bath film forming agent for preventing bouine mastitis and a preparation method of the medicated bath film forming agent, belonging to the field of veterinary medicaments. The medicated bath film forming agent consists of iodine, chlorhexidine acetate, potassium iodide, potassium iodate, glycerol, propylene glycol, polyvinylpyrrolidoneK17, polyvinyl alcohol 17-88, ethanol and distilled water. The medicament has the broad-spectrum bactericidal function, and is dried for 3-5min after being used so as to form a film which is continuous, uniform, firm, has bactericidal activity, flexibility, extensibility, elasticity, abrasion resistance and water resistance, so that the medicated bath film forming agent effectively prevents pathogenic bacteria and virus from entering the mammary gland from a nipple, is safe, non-toxic, non-reactive and non-irritant, can avoid injury of the nipple function due to long-term use, and is a good medicament for preventing bouine mastitis.
EP1569659A2 Dioxolane thymine and combinations for use against 3tc/ azt resistant strains of hiv The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R1 is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group, for use in the treatment of HIV infections which exhibit resistance to 3TC and/or AZT. Preferably, compounds according to the present invention are combined with at least one anti-HIV agent which inhibits HIV by a mechanism other than through the inhibition of thymidine kinase (TK). These agents include those selected from among nucleoside reverse transcriptase inhibitors (NRTI), non-nucloeoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, among others. These agents are generally selected from the group consisting of 3TC (Lamivudine), AZT (Zidovudine), (-)-FTC, ddI (Didanosine), ddC (zalcitabine), abacavir (ABC), tenofovir (PMPA), D-D4FC (Reverset), D4T (Stavudine), Racivir, L-D4FC, NVP (Nevirapine), DLV (Delavirdine), EFV (Efavirenz), SQVM (Saquinavir mesylate), RTV (Ritonavir), IDV (Indinavir), SQV (Saquinavir), NFV (Nelfinavir), APV (Amprenavir), LPV (Lopinavir), fuseon and mixtures thereof. The TK dependent agents, such as AZT and D4T, may be used in combination with one of the dioloxane thymine compounds according to the present invention, but the use of such agents may be less preferred. In preferred compositions according to the present invention, Rl is preferably H or a C2-C18 acyl group or a monophosphate group. Pharmaceutical compositions and methods of reducing the likelihood that a patient at risk for contract an HIV infection will contract the infection are other aspects of the present invention.
EP1905446A1 Use of PYY analogs and antagonists of PPY receptors for manipulating satiety The present invention relates to uses of peptide YY, a peptide YY functional analog or an antagonist of receptors for peptide YY for manipulating satiety in mammals. Peptide YY or a peptide YY functional analog may be used for inducing satiety whereas antagonists of receptors for peptide YY may be used for suppressing satiety in mammals.
US20130071458 Active agents and their oligomers and polymers Conjugates comprising at least two active agents linked by a diglycolic acid or polyglycol diacid linker are disclosed. The invention also concerns oligomers and polymers of these conjugates and their use in therapeutic and industrial applications for localized, immediate or fast release delivery of an active agent, such as an anti-microbial, anti-infective, or antiseptic agent.
EP2331096A1 Dabigatran in tumour therapy The invention relates to the use of dabigatran etexilate of Formula (I) optionally in the form of the pharmaceutically acceptable salts thereof, as well as new medicament formulations for the treatment of tumours.
US20080247955 Detecting secreted phosphoprotein-1 and/or biomarkers; autoimmune diseases; antibodies; RNA interference The present invention provides methods of treating inflammatory diseases/disorders in a subject by inhibiting/antagonizing TREM-1 expression/activity/signal transduction and/or DAP12/TyroBP expression and/or activity. Methods of detecting the presence of inflammatory disease in a subject by detecting TREM-1 and/or DAP12/TyroBP expression and/or activity in the subject or a sample obtained therefrom, wherein increased expression or activity is indicative of the inflammatory disease are also included. The present invention further provides methods for assessing the efficacy of a TREM-1-modulating agent administered to a patient by detecting levels of secreted phosphoprotein 1 (SPP1) and/or one or more other biomarkers in the patient or in a sample from the patient.
WO2013021138A2 Yeast flakes enriched with vitamin d2, compositions containing same, method for preparing same, uses thereof, and device for implementing the method The invention relates to yeast flakes enriched with vitamin D2, to compositions including said flakes, and to the uses thereof, as well as to a method for preparing yeast flakes enriched with vitamin D2 and to the device for implementing same.
WO2006013960A1 Salts of benzimidazole derivative with amines and process for production thereof The invention provides (1) a process for the production of alkali metal salts of 2-[{4-(3-methoxypropoxy)-3- methylpyridin-2-yl}methylsulfinyl]-1H-benzimidazole which are useful as gastric acid secretion inhibitor, antiulcer agent, and other drugs and (2) salts of 2-[{4-(3-methoxypropoxy) -3-methylpyridin-2-yl}methylsulfinyl]-1H- benzimidazole with amines which are intermediates for the production of the alkali metal salts and a process for the production of the same. Specifically, salts represented by the general formula (Ι): wherein A+ is an isopropylammonium ion, a sec-butylammonium ion, or a cyclopentylammonium ion.
US7196195 8-chloro-6,11-dihydro-11-(4-piperidilydene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine); good solubility; anti-allergen The object of the present invention are new desloratadine salts of formula I wherein the meaning of X is an acid residue and the meaning of n is 1 or 2, and formula II wherein the meaning of X is a pK <3.5 acid residue. The invention is related to a process for their synthesis, as well as new anti-allergic pharmaceutical compositions containing these salts
EP1722778A1 Methods and compositions for the treatment of lipodystrophy The present invention is directed to methods and compositions for the treatment of lipodystrophy. The methods contemplate treatment of lipodystrophy in both HIV and non-HIV patients. More specifically, the methods are directed to a combination therapy that employs growth hormone and statins to effect treatment of lipodystrophy.
CN103509006A Flumatinib mesylate crystal form, and preparation method and use thereof The invention discloses a flumatinib mesylate crystal form, and a preparation method and a use thereof. XRD characteristic peaks of the flumatinib mesylate crystal form are shown as in figure 1 in the specification. The preparation method of the flumatinib mesylate crystal form comprises the following steps: dissolving flumatinib mesylate in acetone, crystallizing at 0-10DEG C, and filtering to obtain the target crystal form.
EP1542972A2 Cyclooxygenase- 2 selective inhibitors, compositions and methods of use The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endotheliumderived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
WO2008023455A1 Tyrosinase inhibitor Disclosed is a tyrosinase inhibitor which has excellent tyrosinase-inhibiting activity, is safe and inexpensive, and is useful as a pharmaceutical, a cosmetic, a food or a food additive. The tyrosinase inhibitor comprises a triacyl glycerol represented by the general formula (1) as an active ingredient. (1) wherein R1, R2 and R3 independently represent a linear fatty acid residue having 10 to 18 carbon atoms.
CN102861056A Application of Houttuynoid A in endometrial cancer treatment medicine The invention relates to application of Houttuynoid A in preparing endometrial cancer treatment medicine, which belongs to the technical field of new application of the medicine. According to the assessment on the antineoplastic activity through in-vitro MTT method, Houttuynoid A has an obvious inhibiting effect on the growth of human endometrium cancer cell strains ISK and RL95-2. Therefore, Houttuynoid A can be used for preparing the endometrial cancer treatment medicine, and has a favorable development and application prospect. The application of Houttuynoid A in preparing the endometrial cancer treatment medicine, which is provided by the invention, is disclosed for the first time, and because the skeleton type belongs to brand-new skeleton type, the inhibiting activity of HouttuynoidA to endometrium cancer cells is extremely strong.
US6939862 Method for transferring nucleic acid into striated muscles The invention provides a method of transferring in vivo a molecule into a striated muscle cell. More specifically, a method of the invention comprises contacting in vivo a striated muscle cell with a molecule, and electrically stimulating the muscle cell with one or more unipolar pulses of an electric field intensity ranging from 1 to 800 V/cm2. In one embodiment, the molecule is a nucleic acid encoding a protein of interest. For example, the invention provides methods of promoting angiogenesis and hemostasis.
CN101085758A 1-arylmethyl-3-aryl-1H-pyrazole-5-carbohydrazide derivative, preparation method and application thereof The invention relates to 1- aryl methyl- 3- arylamine - 1H- pyrazole- 5- carbonhydrazides derivant in general formula (I). R1 represents hydrogen, alkyl group of C1 to C4, alkoxy, halide or nitro; R2 represents hydrogen, alkyl group of C1 to C4, alkoxy, halide or nitro; X represents carbon or nitrogen. The invention aslo relates to a method for synthesizing, separating and purifying said compound. Said method comprises following steps: taking aryl chloride and 3- arylamine - 1H- pyrazole- 5- ethyl formate as raw material, refluxing it in polar solution with potash existence and preparing derivant of 1- aryl methyl- 3- arylamine - 1H- pyrazole- 5- carboxylate, mixing said derivant with hydrazine hydrate in polar solution for reaction and getting 1- aryl methyl- 3- arylamine - 1H- pyrazole- 5- carbonhydrazides derivant. The invention aslo relates to the application of said product for preparing medicine for promoting lung carcinoma A549 cell withering.
US20110178062 Indole and benzothiophene compounds as modulators of the histamine h3 receptor Certain substituted indole and benzothiophene compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
WO2014003849A1 USE OF 2-METHYLENE-19-NOR-(20S)-1α,25-DIHYDROXYVITAMIN D3 TO TREAT SECONDARY HYPERPARATHYROIDISM Disclosed is the use of 2-methy1ene-I9-nor-(20S)-lα,25-dihydroxwitamin D3 to treat and/or prevent secondary hyperparathyroidism and/or its accompanying symptoms in a subject having or at risk for developing secondary hyperparathyroidism without inducing hypercalcemia in the subject.
CN101797238A Method for preparing medicinal preparation for releasing rifampicin on upper part of small intestine and characteristics of medicinal preparation The invention discloses a method for preparing a medicinal preparation for releasing rifampicin as an anti-tuberculous first-line medicament on the upper part of small intestine and characteristics of in vitro medicament dissolution and in vivo release and absorption which the medicinal preparation should have. The method is characterized in that: the weight increment of a micro-pellet enteric coating material is between 1 and 9.9 percent; the weight increment of a granular enteric coating material is between 1.5 and 10.9 percent; the weight increment of a micro-tablet enteric coating material is between 0.5 and 8.9 percent; a release and absorption curve of a rifampicin micro-pellet in vivo should show that the blood medicament concentration is 16+/-0 to 26 percent of a peak value of the blood medicament concentration within 20 minutes after oral administration and is 23 to 77 percent of the peak value of the blood medicament concentration within 40 minutes; and during a time interval between 20 and 40 minutes, a rising speed of the blood medicament concentration is 0.63 to 2.73 percent of that of the peak concentration.
CN102614213A Application of glycyrrhizic acid, glycyrrhetinic acid or salt thereof as well as gel composition and preparation method for gel composition The invention aims to provide an application of glycyrrhizic acid, glycyrrhetinic acid or salt thereof in preparation of medicines for locally preventing and treating radiodermatitis so as to solve the problem of low effective rate of the conventional anti-radiodermatitis method, and further provides a preparation method for glycyrrhizic acid, glycyrrhetinic acid or salt and chitosan mixing composition according to the application. Compound biological gel prepared by the method has better therapeutic effect compared with that of the conventional anti-radiodermatitis medicine, has the radiodermatitis-preventing effect which the conventional medicine does not have, and is safe, non-toxic and non-irritant for a human body.
WO2012171488A1 Coumarin derivative, pharmaceutical composition and use thereof The present invention relates to a coumarin derivative of formula (I): wherein X, Y1, Y2, Y3, R1, R2, R3 and R4 are as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising the compound of the present invention, and use of the compound of the present invention in treating tumor and/or inflammation.
WO2013041038A1 Pyridine compounds as inhibitors of kinase Disclosed are pyridines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions.
US20080200433 Molecular Chaperone Function Regulator According to the present invention, a molecular chaperone function regulator containing a quinazoline derivative represented by the following formula (I) wherein each symbol is as defined in Claims, or a pharmaceutically acceptable salt thereof, a hydrate or solvate thereof, an optically active form or racemate thereof or a diastereomer mixture thereof as an active ingredient can be provided.
CN101270102A Process for synthesizing parthenolide derivative and uses thereof The present invention relates to a synthetic method of derivatives of parthenolide lactone. Parthenolide lactone and nitrogen-containing compounds are used as the raw materials of the reaction; ethanol sodium is used as a catalyst; the mixture reacts in a certain solvent and at a certain temperature; thus the derivatives of the parthenolide lactone can be prepared. After acidification, the salts of the derivatives can be prepared with greatly improved water solubility. The improved salts of the derivatives of the parthenolide lactone can be used for preparing injection so as to better treat tumors.
CN101018782A Hydantoin compound for the treatment of inflammatory disorders This invention relates to compounds of Formula (1) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAM, TACE, TNF- or combinations thereof.
WO2008131547A1 'triazine derivatives, compositions containing such derivatives, and methods of treatment of cancer and autoimmune diseases using such derivatives' We describe compounds of the following general formula (I): wherein X is fluorine or chlorine; Y is oxygen, sulfur, or an amino group; R is an amino, hydroxyl, sulfonamide, or carboxamide group or an N-monomethyl or N-dimethyl analog thereof; m is an integer from 2 to 6, and n is an integer from 0 to 2. The compounds may be used for treating certain cancers and autoimmune diseases.
EP2708145A1 Methods for modulating corticosterone levels in psychologically stressed individuals Disclosed are methods of modulating and/or decreasing serum corticosterone levels in an individual affected by stress. Further disclosed are methods of modulating the hypothalamic pituitary adrenal response in an individual. The methods include administration of 2-fucosyl-lactose to an individual.
CN103265476A Azasugar quaternary ammonium salt compound and preparation method and application thereof The invention discloses an azasugar quaternary ammonium salt compound and a preparation method and application thereof. The structure of the azasugar quaternary ammonium salt compound is shown in formula I described in the specification. The preparation method for the azasugar quaternary ammonium salt compound is simple; and the azasugar quaternary ammonium salt compound can be used for glycosidase inhibitors, medicaments for preventing and/or treating diabetes, medicaments for preventing and/or treating Gaucher disease, medicaments for preventing and/or treating tumors and anti-virus medicaments.
CN103209967A Meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide A preparation replete with a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
WO2010078307A1 Spiro-oxindole-derivatives as sodium channel blockers This invention is directed to spiro-oxindole compounds of formulas (I), (II), (III), as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel -mediated diseases or conditions, such as pain.
CN102793690A Application of juglone to preparation of medicament for treating autoimmune and inflammatory diseases The invention discloses an application of juglone to preparation of a medicament for treating autoimmune and inflammatory diseases. As proved by an experimental result, the juglone can be used for lowering the disease incidence, average clinical score, highest clinical score and total clinical scores of mouse experimental autoimmune encephalomyelitis, lowering the percentages of an IFN (Interferon)-gamma secretion-relevant cell Th1 and a 1L-17A secretion-relevant cell Th17 in spinal marrow of mouse experimental autoimmune encephalomyelitis in a CD4+T cell, inhibiting the proliferation of a cell T induced by MOG (Myelin Oligodendrocyte Glycoprotein) of the mouse experimental autoimmune encephalomyelitis, and lowering the expression of CD11b+ angtigen presentation cells CD83 and MHCII in the spleen of the mouse experimental autoimmune encephalomyelitis. The juglone for preparing a medicament for inhibiting an immune system related to the invention is expected to become a medicament for clinically treating autoimmune inflammatory diseases such as multiple sclerosis, acute disseminated encephalomyelitis and the like.
CN102058613A New application of antineoplastic constituent compound in solanum nigrum The invention relates to the application of ratio compounds of two simplex components in plant solanum nigrum extracts to preparing medicaments for treating liver cancer.
EP2442650A1 Sublingual apomorphine The invention features sublingual formulations of apomorphine and apomorphine prodrugs, and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.
WO2011058027A3 N-9-substituted purine compounds, compositions and methods of use The present invention relates to compounds of Formula (I), wherein R1, R2, R3, A1, A2, A3, A4 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses against cancer via inhibition of mTOR and PI3K.
US20100263065 Materials and methods for gene mediated therapy of psychiatric disorders The invention provides materials and methods for p11-mediated therapy of psychiatric disorders. The invention provides vectors for increasing p11 expression and methods of treating a mammal with one or more symptoms of a psychiatric disorder. The invention also provides methods for improving a mammal's responsiveness to treatment for a psychiatric disorder. The invention further provides model animals for depression and depression therapy.
CN101735286A Amino acid modified glucosamine as well as preparation method and application thereof The invention discloses an amino acid modified glucosamine shown as the general formula I. By detection, the amino acid modified glucosamine has more favorable PPAR agonist activity and potential and wide application prospect in the field of treatment of diabetes, is a favorable diabetes resistant leading compound and can be further developed to prepare a diabetes resistant medicament. The invention also provides a preparation method of the amino acid modified glucosamine. An intermediate 2-amino-1,3,4,6-four-O-beta-D-glucosamine sulfate is synthesized in one step by adopting 2-amino-beta-D-glucosamine hydrochloride as an initial raw material through an improved acetic anhydride-sulfuric acid method, and the intermediate is coupled with protected amino acid under the action of a condensing agent to obtain the amino acid modified glucosamine. The invention has short reaction step, mild reaction condition, convenient postprocessing, high yield and low cost.
US7012079 (5R)-5-ethyl-9,10,difluoro-5-hydroxy-12-(2-trimethylsilylethyl)-4,5,13,15-tetrahydro-1H,3H-oxepino[3',4':6,7]-indoloizino[1,2-b]quinoline-3,15-dione for treatment of colon cancer The invention relates in particular to the compounds of general formula in which R1, R2, R3, R4, R5, R6 represent various radicals; their use as medicaments and pharmaceutical compositions containing them. These compounds are particularly useful for the treatment of cancer.
US20060019344 C-erbB-2 external domain: gp75 Disclosed are methods and compositions for identifying malignant tumors that overexpress the c-erbB-2 oncogene. Assays useful for diagnosis and prognosis of neoplastic disease are provided which detect the external domain of c-erbB-2, the glycoprotein gp75 and quantitate the level of gp75 in the biological fluids of mammals carrying a tumor burden. Further disclosed are recombinant, synthetically and otherwise biologically produced novel proteins and polypeptides which are encoded by the external domain DNA sequence of the c-erbB-2 oncogene (the gp75 gene) or fragments thereof. Such gp75 proteins and polypeptides are useful as vaccines, therapeutically in the treatment of cancer either alone or in combination with chemotherapeutic agents. Also disclosed are antibodies to such gp75 proteins and polypeptides which are useful diagnostically and therapeutically. Still further disclosed are test kits embodying the assays of this invention.
CA2305803C Crystalline antifungal polymorph The crystalline polymorph Form I of (-)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-yl-methyl)furan-3-yl]methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one represented by formula (I), pharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed.
US20090176806 protein kinase C or glycogen synthase kinase-3-beta inhibitors such as 3-(2-chlorophenyl)-4-[1-(3-hydroxypropyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-1H-pyrrole-2,5-dione, used for treating cardiovascular, skin, nervous system disorders and immunological disorders, diabetes, inflammatory diseases and cancer The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.
EP1511774A1 Per (3,6-anhydro) cyclodextrin derivatives, their preparation and use thereof for separating ions, in particular chromium and manganese anions The invention concerns per (3,6-anhydro) cyclodextrin derivatives comprising in C2 at least one carbamate group, polymers thereof, their preparation and their use for separating anion contaminants, such as CrO4<2->, Cr2O7<2->, MnO4<-> anions.
EP1395590B1 Dihydropyrrolo¬1,2-a|indole and tetrahydropyrido¬1,2-a|indole derivatives as prostaglandin d2 receptor antagonists Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
CN102166302A Metabolism-compensation method for treating rheumatic osteoarthritis and proportioning and preparing process of preparation thereof The invention relates to a metabolism-compensation method for treating patients with rheumatic joint diseases by pure natural plant extracts. By adopting a molecule shearing technology, a technology for promoting the metabolic turnover of body tissues and a gene recombination technology, according to the latest outcomes of gene expression and immune response, the traditional process and a high-tech biotechnology are combined to prepare orally taken and externally applied preparations, a physical or chemical constant-temperature auxiliary treatment instrument is used for maintaining the optimal enzyme synthesis and enzyme decomposition temperature (36-38 DEG C) in body cells, and medicinal and edible ways are used for compensating substances required for body metabolism to promote secretion of hyaluronic acids in synovia of parts such as knees, ankles, wrists, elbows, shoulder blades, lumbar vertebrae and the like and promote metabolic normalization of joint cartilage, thereby economically and efficiently treating arthritic patients, inducing the regeneration of the inflammatory joint synovium, tendon, ligament and cartilage, promoting the self-renewal of synovial fluid, removing inflammatory blood stasis, relieving pain, preventing cartilage tissues from being damaged, preventing the distortion of articular bones, and finally treating patients with rheumatic bone diseases thoroughly.
WO2012100017A2 Antiretroviral cyclonucleoside compositions and methods and articles of manufacture therewith Aspects of embodiments relate to methods of treating human immunodeficiency virus (HIV) infection. Further aspects of embodiments also relate to constellations of compositions for treating HIV infection. Still additional aspects of embodiments relate to a many methods of making compositions useful in the treatment of HIV infection.
CN101502515A Hydrochloride loratadine enteric-coated formulation composition and method for preparing the same The invention discloses a lorapadine hydrochloride enteric preparation combination and a preparation method thereof. The lorapadine hydrochloride enteric preparation combination is mainly prepared from lorapadine hydrochloride bulk drugs and appropriate auxiliary materials. Compared with the common lorapadine hydrochloride preparations, the lorapadine hydrochloride enteric preparation provided by the invention has the advantages that the lorapadine hydrochloride enteric preparation is less irritant to the stomach, thereby reducing the adverse reactions. The lorapadine hydrochloride enteric preparation combination is particularly suitable for patients with stomach-upset diseases. The invention provides a novel form of drug featuring higher safety and better curative effect and having the advantages of high quality controllability and stability of the preparation process.
US20120149708 Modulators of viral transcription, and methods and compositions therewith The present invention is directed to a process for inhibiting the replication of human immunodeficiency virus-1 (HIV-1), by contacting a cell with at least one compound according to Formula I. The substituent groups R1, R2, R3, X, Y, Z, A and B are as defined above. Also contemplated is a method for treating or preventing a HIV-1 infection in a subject, by administering a therapeutically effective amount of at least one compound according to Formula I, as well as a method for modulating the activity of a cyclin dependent kinase (cdk) in a cell infected with HIV-1 using a Formula I compound.
CN1628645A Ambroxol hydrochloride oral disintegrating tablet and preparation method thereof The invention discloses an ambroxol hydrochloride oral disintegrating tablet and preparation method, wherein the tablet is for treating acute, chronic respiratory diseases, the invention provides a novel dosage type and a novel method for administration which comprises, placing medicament onto tongue, dissolving when meeting ptysma, acting by means of swallowing movement, the medicine is convenient for a plurality of groups of people, such as the elderly, children, or patients of dysphagia or in special environment.
EP1112255B1 4,4-biarylpiperidine derivatives with opioid receptor activity The present invention relates to compounds of formula (I), wherein Z?1, Z2, R1, R2 and R3¿ are defined as in the specification, pharmaceutical compositions containing such compounds, the use of such compounds to treat neurological and gastrointestinal disorders.
CN1911211B Solid oral preparation of leishajilan An orally taken solid of rasagiline with high disintegrating speed in oral cavity is proportionally prepared from rasagiline or its pharmacologic salt, filler and disintegrant.
US7199243 Antilipemic agents; anticholesterol agents; atherosclerosis; cardiovascular disorders; obesity; antidiabetic agents PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.
CN103271836A Non-cytotoxic chlorine dioxide fluids Disclosed are compositions related to a substantially non-cytotoxic chlorine dioxide solution. The solution may be a thickened fluid composition. Also disclosed are methods of making and using a substantially non-cytotoxic thickened fluid compositions or solutions comprising chlorine dioxide solution. An oxidizing composition of reduced irritation is also disclosed.
CN102018823A Composite preparation containing phospholipid, alpha-linolenic acid, gamma-linolenic acid and tomato extract The present invention relates to a composite preparation containing phospholipid, alpha-linolenic acid, gamma-linolenic acid, tomato extract, phytosterol, etc. The composite preparation can be used to prepare health food, medicine and functional food that have the functions of treatment and prevention to cardiovascular diseases and prostate diseases, the alleviation of age-related awareness decrudescence, the improvement of memory, the relief of cerebral fatigue, the alleviation of mental pressure, and the improvement of childhood hyperkinetic syndrome. The composite preparation can be prepared into dosage forms of soft capsules, dropping pills, etc. which are convenient in administration and easy to popularization.
US20110275698 "test and treat" strategy for treating transforming hpv infection The invention is concerned with a “test and treat” method of screening and directly treating female subjects having transforming or abnormal human papillomavirus (HPV) infection.
US20120003181 Novel Retinoid Inducible Factor and Uses Thereof The present invention describes a novel retinoid-responsive nucleic acid, and a novel protein. Further, the invention describes the use of such a nucleic acid or protein in various diseases, and for the treatment, the diagnosis and prognosis of various diseases, and also for a method for the prognosis of responsiveness to retinoids.
WO2007065683A1 Aryl acetic acid and ester derivatives and their uses as antiinflammatory There are provided according to the invention compounds of formula (I), in free or salt form, wherein R1, R2, R4, R5, R6, A, D, X, W, m and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.
WO2009151393A1 Novel derivatives of 11-piperazin-l-yldibenzo [b,f] [l,4] thiazepine for treating at least one syndrome or condition associated with schizophrenia and other psychotic disorders This invention relates to novel compounds having the structural Formula I below: (I) and their pharmaceutically acceptable salts, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence, and neurodegenerative disorders.
WO2010053388A1 New 4,6-disubstituted 2-(4-methylpiperazin-1-yl)pyridine derivatives, a process for their preparation, pharmaceutical composition containing these compounds, their use, a method for modulating monoaminergic receptor activity and a monoaminergic receptor modulating agent The subjects of the invention are new 4,6-disubstituted 2-(4-methylpiperazin-1-yl)pyridine derivatives, a process for their preparation, pharmaceutical composition containing these compounds, their use, a method for modulating brain monoaminergic receptor activity and a monoaminergic receptor modulating agent. The invention relates to new chemical compounds, 2-(4-methylpiperazin-1-yl)pyridine derivatives, enantiomers thereof or a mixture of its enantiomers or their pharmaceutically permissible prodrugs and salts, pharmaceutical compositions containing these compounds, and methods of using any of these derivatives and compositions for the prevention or treatment of neurological or psychiatric diseases, especially related with the modulation or regulation of brain monoaminergic receptors such as serotonin receptors, preferably receptors selected from the group of: 5-HT6, 5-HT2A, 5-HT7, dopamine receptors, preferably D2 and adrenergic receptors, preferably α. These new compounds can be used for treating central nervous system diseases.
WO2010119984A1 3-aryl or heteroaryl-substituted indole derivative A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Y1 and Y2 both represent a hydrogen atom or Y1 and Y2 together form -CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al.
WO2011149601A1 Treatment of vagally- mediated spectrum disorders with 5ht3 antagonists The present invention provides a treatment of a vagally-mediated spectrum disorder, comprising administering an effective amount of a 5-HT3 receptor antagonist to a patient in need thereof.
CN101302184A Indoline sulfanilamide compound The present invention provides an indoline sulfanilamide compound shown in the formula (I), wherein, R is hydrogen or halogen; R<2> is Ar, Ar-C(O)-, Ar-CH2-, Ar-SO2-, Ar-O-C(O)-, (see FIG) or R''-C(O)-, wherein Ar is aryl, cyclic radical, heterocyclic radical or heteroaryl of C5-C20 which is substituted or not substituted, R' and R'' respectively are alkyl of C1-C10 and alkoxy of C1-C10; and R3 is aryl of C5-C15 and alkyl of C1-C10.The compound also can be used with a pharmaceutically acceptable carrier to form a medicine composition for restraining the polymerization of a microtubule in a cell, or for restraining cancers related to the microtubule polymerization.
US20090012015 Large dose ribavrin formulatons The present invention is related to pharmaceutical dosage forms of ribavirin which are designed to increase patient compliance to a ribavirin therapy. Examples of such dosage forms include 400 mg to 600 mg tablets. These dosage forms are bioequivalent to multiple doses of tablets containing small amounts of ribavirin.
US20130040894 Inhibition or activation of serine/threonine ulk3 kinase activity The present invention relates to human serine/threonine kinase ULK3 and its ability to regulate GLI transcription factors; mediators of SHH signaling. This disclosure demonstrates that ULK3 enhances endogenous and over-expressed GLI1 and GLI2 transcriptional activity in cultured cells, and ULK3 alters subcellular localization of GLI1. According to this disclosure ULK3 is an autophosphorylated kinase and phosphorylates GLI proteins in vitro. A peptide sequence in GLI1 C-terminus that is phosphorylated by ULK3 is provided in this disclosure. ULK3 catalytical activity is shown to be crucial for its function in SHH pathway. This disclosure shows that serine/threonine kinase ULK3 is involved in the SHH pathway as a positive regulator of GLI proteins. Furthermore, a therapeutic method in SHH dependent human disorders is disclosed by pharmacological inhibition of ULK3 kinase activity. Identification of ULK3 substrate sequence in GLI1 allows the design of peptide-based modulators of its kinase activity.
US7772209 Antifolate combination therapies A method of administering an antifolate to a mammal in need thereof, comprising administering an effective amount of said antifolate in combination with a methylmalonic acid lowering agent.
WO2013036031A3 Pharmaceutical composition including a microrna486 expression inhibitor as an active ingredient for preventing and treating neurological disorders The present invention relates to a pharmaceutical composition including a miRNA486 expression inhibitor as an active ingredient for preventing and treating neurological disorders. More particularly, since it has been verified that interference with the expression of miR486 using an miR486 inhibitor overcomes the inhibition of NeuroD6, thereby inducing improvements in spinal cord injuries (SCI), the miR486 inhibitor can be used as an active ingredient in a pharmaceutical composition for preventing and treating neurological disorders, and further, the mechanism by which miR486 controls the expression of NeuroD6 can be applied in screening for candidate materials for preventing and treating neurological disorders.
WO2013104399A1 Topical pharmaceutical compositions comprising bexarotene and a corticosteroids Topical pharmaceutical compositions are described comprising: a) bexarotene, b) a corticosteroid, and c) a carrier or vehicle. Said compositions are useful for the treatment of skin disorders.
WO2006105697A1 Piperidyl-2, 6-dione derivatives used to inhibit cells from releasing tumor necrosis factor The present invention is directed to piperidyl-2,6-dione derivatives of formula (I) and inorganic or organic acid salts thereof, methods of producing these compounds, and the use of the compounds as active ingredient in medicine to inhibit cells from releasing TNFα: (I) Wherein, n represents 1, 2, 3, 4, 5, or 6; R1 represents F, Cl, Br, C1-4alkyl, OH, OC1-4alkyl, NO2, NHC (O) C1-4alkyl, NH2, NH (C1-4alkyl), N (C1-4alkyl)2, there are 1-4 R1 and each R1 may be the same or different; R2 represent OR3, NR3R4, N(R3)COR4, O2CR5, wherein R3 or R4 represents H or C1-4alkyl, R5 represents CHR6NR7R8, CHR6NR9C(O)CHR10NR7R8, heterocycle W or CHR6NR9C(O)W, where R6, R9, R10 independently represents H or C1-4alkyl, R7 and R8 independently represents H or C1-4alkyl or R7 and R8 together represent 1,3-propilidene, 1,4-butylidene, 1,5-pentamethylene, 1,6-hexamethylene, W represents four-, five-, six-, seven-, or eight-membered saturated or unsaturated heterocycles.
CA2755590A1 Triazole derivatives as vasopressin-receptor inhibitors for treating cardiac insufficiency The present application relates to novel substituted phenylalanine derivatives, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
CN101353361A Preparation of adriablastina prodrug and use thereof The invention provides a method for preparing a precursor drug of doxorubicine and the application thereof; in the method of the invention, DDC is added in the doxorubicine and Alpha-linolenic acid at room temperature so as to carry out synthesis under the catalysis of DMAP for obtaining the precursor drug of doxorubicine. The precursor drug can improve the anti-tumor effect of the doxorubicine, reduce the side-effects of drugs, and enhance the targeting properties, thereby providing a new idea for developing the anti-tumor drugs.
WO2010059771A1 Substituted pyrrolo[2,3-b]-pyridines and-pyrazines Compounds of Formula I, as shown below and defined herein:(I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.
WO2013014629A1 Pharmaceutical compositions comprising pyrrole diones and their use to inhibit angiogenesis The present invention relates to the use of compounds as angiogenesis inhibitors in the manufacture of a medicament for use in the treatment of disease states associated with angiogenesis, and anti-angiogenic pharmaceutical compositions containing them as active ingredient.
US7888504 Glucokinase activators and methods of using same Compounds are provided which are glucokinase activators and thus are useful in treating diabetes and related diseases and have the structure wherein in the ring represents one or two double bonds; R1 is aryl or heteroaryl; R2 is halogen, cycloalkyl, heterocyclyl, aryl, or heteroaryl; R5 is as defined herein; Z is O, S, S(O), S(O)2, or NR5a; X is S, O, N, NR3, or CR3; Y is NCR4 or N4; R3, R4, and R5 are as defined herein; R8 is aryl or heteroaryl; R6 and R7 are independently H, halogen, or alkyl; m is 0 or 1; and n is 0 to 3, or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
EP1951228A2 Bicyclic spirohydantoin cgrp receptor antagonists Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
CN101412741A Composition with methylprednisolone palmitate as active component for treating local inflammation The invention relates to a drug composition for treating local inflammation, which uses methylprednisolone palmitate as an active composition. The drug composition consists of the methylprednisolone palmitate as the active composition and an inactive composition suitable for local injection, and is used for treating local inflammation of people or mammal through local injection.
US7396946 Compound for treatment of external secretion disorders Disclosed is a method for treatment of external secretion disorders, which comprises administering a fatty 5 acid derivative to a subject in need of said treatment. The method of the present invention is useful for treatment of at least one condition selected from hypolacrimation including disorder of basal tear secretion, dry-eye syndrome, hyposalivation and dry-mouth syndrome.
CN103588782A Gambogellic acid as well as preparation method and application thereof to medicines The invention relates to a caged polyprenylated xanthones compound, namely gambogellic acid, which has the anti-tumor activity. The invention also relates to a preparation method of the gambogellic acid. The preparation method comprises the following steps: with gambogic acid as a raw material, heating and carrying out preparative liquid chromatography separation, thus obtaining the gambogellic acid. The invention also relates to the application of the gambogellic acid to the preparation of anti-tumor medicines.
EP2432328A1 Fat blends and uses thereof A fat blend comprises alpha-linolenic acid, conjugated linoleic acid and oleic acid. The fat blend comprises: (i) greater than 3 % by weight alpha-linolenic acid; (ii) greater than 12 % by weight conjugated linoleic acid; and (iii) greater than 20 % by weight oleic acid, the percentages being based on the total weight of C16 to C20 fatty acids in the blend. The fat blend may be used for increasing the levels of docosahexaenoic acid in the blood of a subject after oral consumption.
US20120214821 Lipidomic Biomarkers of Diabetes The invention, in some aspects, relates to methods for predicting a subject's risk of developing a glucose-related metabolic disorder, e.g., diabetes. In some aspects, the invention relates to methods for selecting and monitoring a treatment for a glucose-related metabolic disorder, e.g., diabetes.
US20100160227 Signaling peptides The present invention provides novel peptides of specified sequence and their use as a signal peptide or a membrane-anchoring peptide. It also relates to chimeric polypeptide comprising one or more such peptides and a polypeptide of interest as well as nucleic acid molecules, vectors, infections vital particles and host cells encoding such peptides and chimeric polypeptides. The present invention also relates to a pharmaceutical composition comprising such elements and a pharmaceutically acceptable vehicle. The present invention also provides a method for recumbently producing a polypeptide using such peptides, especially for directing expression of a polypeptide of interest extracellularly or anchored at the surface of the plasma membrane.
CA2648126C Treatments using citrulline The invention provides a method and formulation for the treatment or maintenance of conditions that would be benefited from increasing or maintaining Arginine levels in the blood, and having improved taste characteristics over current Arginine supplementations. Further, this maintenance of Arginine levels in the blood will be beneficial in acute and chronic diseases with an impaired arginine to citrulline production rate. Further the invention provides a method for treating at least one of satiety and dyspepsia in an individual. In one embodiment, the method includes administering to an individual an effective amount of L-citrulline.
CN103006622A New borneol use and lung cancer treatment drug composition The present invention belongs to the field of medicine, and specifically relates to a new borneol use and a lung cancer treatment drug composition. The first technical problem solved by the present invention is a use of borneol in anticancer drug preparation. The second technical problem solved by the present invention is to provide a completely new lung cancer treatment drug composition, which comprises borneol and cyclophosphamide. Test results show that single use of the borneol provides a lung cancer inhibition effect, combination of the borneol and the cyclophosphamide provides an increased tumor inhibition rate, and improvement of leukocyte inhibition by the cyclophosphamide is further provided. With the present invention, a completely new, safe and efficient selection is provided for clinical lung cancer treatment.
WO2010086040A1 Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy Compounds of formula (I) wherein R1, R2, R3, R4, R5, L1, L2, m, and n are as defined herein, are useful for the treatment or prophylaxis of conditions such as Duchenne muscular dystrophy, Becker muscular dystrophy, and cachexia.
WO2009020192A1 Composition for oral intake for preventing ultraviolet damage It is intended to provide a composition for oral intake which can effectively prevent skin damage induced by the exposure to ultraviolet light when orally taken. This problem can be solved by a composition for oral intake for preventing ultraviolet damage characterized by containing a composition obtained from fruits of a Cucumis melo variety, and a composition for oral intake for preventing ultraviolet damage further containing a polyphenol component contained in red wine, a component obtained from pine bark and/or vitamin C. Moreover, the above-described problem is solved by a skin-care product for oral intake, a food and a drink each comprising the composition for oral intake for preventing ultraviolet damage as described above.
EP2440536A1 Oxazole and thiazole derivatives as alx receptor agonists The invention relates to oxazole and thiazole derivatives of formula (I), wherein A, E, X, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
EP1734943A1 Use of capsaicin and capsaicinoids for diagnosing chemical hypersensibility The chemical hypersensibility of the intestine that occurs in many gastro-intestinal disorders can be diagnosed and optionally treated simultaneously using capsaicin and/or capsaicinoids.
WO2005012255A1 Remedy for inflammatory joint diseases It is intended to provide a drug for inhibiting the proliferation and/or migration of synovial cells and a drug for treating and/or preventing inflammatory joint diseases. Namely, a drug for inhibiting the proliferation and/or migration of synovial cells and a drug for treating and/or preventing inflammatory joint diseases comprising, as the active ingredient, a pyrazolone derivative represented by the following general formula (I): (I) its physiologically acceptable salt or a hydrate or a solvate thereof.
US20110098244 Process for Isolating Sialic Acid Containing Oligosaccharides, and the Compositions Containing Sialic Acid Containing Oligosaccharides Obtainable Thereby The invention relates to a process for isolating sialic acid containing oligosaccharides and in particular sialyllactose from a milk stream and especially from a whey stream. The process yields a product having a high content of sialyllactose and a low content of phosphorus compounds. This product is highly suitable to be included in infant foods.
EP2185512A2 Trans-3-aza-bicyclo[3.1.0]hexane derivatives The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
CN1985806A Oral dissolved Brufen tablet and its preparing method The oral dissolved Brufen tablet is prepared through the following steps: dissolving Brufen of 1 weight portions in alcohol or 95 % concentration water solution of alcohol in 1-3 weight portions, adding to 30-50 % concentration water solution of hydrophilic supplementary material in 5-12 weight portions through homogeneous mixing, packing in non-toxic plastic bubble cap, and freeze drying. The oral dissolved Brufen tablet is dissolved and dispersed in oral cavity, and thus has great contact area to gastric wall, lower medicine concentration in stomach, less stimulation to stomach, raised solubility and absorption, less untoward reactions and high curative effect.
CN102657600A Povidone iodine gel for veterinary use and preparation process The invention discloses a formula and a preparation process of povidone iodine gel for veterinary use, and particularly relates to povidone iodine gel for veterinary use and a preparation process. The prescription of the medicament consists of povidone iodine, a moisturizing lubricant, a gel matrix, a stabilizer, buffer solution and sterilized water. According to the preparation process, the PH value and the proportion are adjusted to process the povidone iodine gel. The povidone iodine in the gel has the advantages of high bactericidal power, wide antibacterial spectrum, small stimulus, no allergenicity, low toxicity, no drug resistance, no influence on quality of lactation milk, no milk withdrawal period and insensitivity of a sow to the smell of the gel; after the povidone iodine is prepared into the gel, effective iodine of the povidone iodine is more stable to fulfill the aims of slow release and high efficiency; the moisturizing lubricant is added into the gel, so that the povidone iodine is close to the wall of uterus in the uterus and is easier to absorb; and through the stabilizer and the buffer solution in the gel, the effective iodine is stable, and the influence of external environment is avoided.
WO2007053618A1 Prodrugs of muscarinic agonists and methods of treatment of neuropsychiatric disorders Compounds are described that are prodrugs to active compounds that modulate a muscarinic receptor. In some cases, the compounds are prodrugs to. N-desmethylclozapine. The compounds may be used to treat neuropsychiatric disorders.
CN102240394A Use of interleukin-1receptor antagonist (IL-1Ra), and pharmaceutical compositions of IL-1Ra The invention belongs to the technical field of biomedicine, specifically relates to a use of an interleukin-1receptor antagonist (IL-1Ra), and pharmaceutical compositions of the IL-1Ra. The invention discloses a use of protein selected from the following (a) or (b) in preparing drugs for treating or preventing a cardiac toxic reaction due to chemotherapeutics: (a) amino acid sequence of the protein is represented by SEQ ID NO.1; (b) the protein shares 70% amino acid sequence identity with the protein provided by the (a), and has activities for treating or preventing the cardiac toxic reaction due to the chemotherapeutics. According to the protein provided by the present invention, the cardiac toxic reaction due to the chemotherapeutics can be effectively removed or reduced, and a new selectivity may be provided for the future clinical treatment of tumor.
EP1723957A2 Carbostyril derivatives and serotonin reuptake inhibitors for treatment of mood disorders The pharmaceutical composition of the present invention comprises at least one carbostyril derivative in combination with at least one serotonin reuptake inhibitor.
US7541341 2-(4-ethylbenzyl)-5-hydroxymethylphenyl 6-O-ethoxycarbonyl- beta -D-glucopyranoside; for treatment/prevention of hyperglycemia associated with diabetes/obesity The present invention provides glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein P represents a hydrogen atom or a group forming a prodrug; R1 represents a hydrogen atom, an optionally substituted amino group, a carbamoyl group, an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkylthio group, etc., which have an improved oral absorption, and exert an inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, or pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.
US20120309816 Novel viral vector construct for neuron specific optimized continuous DOPA synthesis in vivo The present invention relates to a one-vector expression system comprising a sequence encoding two polypeptides, such as tyrosine hydroxylase (TH) and GTP-cyclohydrolase 1 (GCH1). The two polypeptides can be should preferentially be expressed at a ratio between 3:1 and 15:1, such as between 3:1 and 7:1. The invention is useful in the treatment of catecholamine deficient disorders, such as dopamine deficient disorders including but not limited to Parkinson's Disease. Moreover, the present invention provides a method to deliver the vector construct in order to limit the increased production of the catecholamine to the cells in need thereof.
US20080260823 Ease of administration for patients who have difficulty swallowing; side effect reduction; drooling prevention; neurological disorders The invention provides an orally disintegrating tablet comprising a therapeutically effective amount of glycopyrrolate for treating sialorrhea, as well as a kit comprising the orally disintegrating tablet, prescribing information, and a container. The invention also provides a method of treating sialorrhea in a patient comprising administering the orally disintegrating tablet comprising a therapeutically effective amount of glycopyrrolate to the patient.
CN101224203A Tanshinone IIA microemulsions and preparing method thereof The invention discloses a tanshinone II A microemulsion preparation which has targeting and comparatively high entrapment efficiency and drug-loading rate, is not haemolytic and mainly applied to the treatment of tumor and a preparation method thereof. The invention comprises the following raw materials by weight percentage: 0.6-0.8 percent of tanshinone II A, 0.6-1.8 percent of phosphotide for injection, 2.5-3 percent of glycerin for injection, 1.5-3 percent of F68 for injection, 11-15 percent of ethyl oleate and water for injection. The preparation method of the invention is that first the tanshinone II A is dissolved in the ethyl oleate to prepare the oil phase mixture solution; next the phosphotide for injection, the glycerin for injection and the F68 for injection are dissolved in the water for injection which accounts for 60-70percent of the total water for injection to prepare the water phase solution; then the oil phase solution and the water phase solution are respectively preheated to 60-70DEG C and the oil phase solution is slowly dropped to the water phase solution when the water phase solution is blended; the mixed solution is then sheared for 1-2minutes in a high shearing dispersing emulsification machine and filtrated with a 0.8Mum filtration membrane when the solution is still hot and the rest water for injection is added to the filtrate; the liquid obtained from step d is homogenized by a high pressure emulsification machine and next filtrated with the 0.8 Mum filtration membrane; finally the filtrate obtained from step e is packaged, filled with nitrogen, sealed and disinfected.
EP2331494A1 A process for the preparation of rotigotine A process for the preparation of Rotigotine (I) and of pharmaceutically acceptable salts thereof, which comprises the reductive amination of an amine of formula 6 with the 2-thienylacetic acid- sodium boron hydride complex and which makes use of hydrobromide 5 as an intermediate (II) The process is advantageous from the industrial point of view in that it allows to obtain Rotigotine with high enantiomeric purity starting from optically active 5,6,7,8-tetrahydro-6-(S)-N-propylamino-l-methoxy- naphthalene (2), avoiding the use of dangerous reactives, the need for difficult chromatographic separation or the formation of by-products. Furthermore, two novel crystalline forms are disclosed.
US20080233188 [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide, a disintegrant, a surfactant, and a lubricant; endothelin receptor inhibitor The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof.
EP1501497A2 Catechin multimers as therapeutic drug delivery agents Described herein are catechin multimers, and particularly substituted catechin multimers, and their use as carrier moieties for the delivery of nucleophilic and cationic bioactive therapeutic agents to target sites in vivo. For example, substituted catechin multimers of the present invention may be administered alone, for the treatment of stenotic vascular diseases and disorders, such as atherosclerosis (also known as arteriosclerosis) and coronary heart disease (also known as coronary artery disease and ischemic heart disease). Alternatively, catechin multimers, substituted and otherwise, may be complexed with nucleophilic and/or cationic bioactive therapeutic agents, such as anti-thrombotic agents, cholesterol lowering agents, anti-plaque agents, anti-cancer agents, chemotherapeutic agents, anti-inflammatory agents, agents antibiotics, antimicrobials, wound healing agents, and the like, for the treatment of a variety of diseases and disorders, including but not limited to cardiac and vascular stenoses, cancer, inflammatory conditions, neurological conditions, infection, wounds, burns and the like. The catechin multimers, particularly the subtituted catechin multimers, described herein have a strong affinity for polar proteins residing in the vascular endothelium as well as cell walls and membranes, and, accordingly, are able to provide targeted delivery of bioactive agents embedded therein and/or complexed therewith so as to potentiate their therapeutic effects. The therapeutic complexes may be pharmaceutically formulated 'neat' (e.g., without additives) or with additives such as pharmaceutical carriers, diluents, buffers, adjuvants, excipients, surfactants, and stabilizers.
WO2007063509A8 Phosphocreatine complexes The invention relates to novel phosphocreatine complexes useful for the treatment of diseases of the central nervous system, having the following general formula (I): wherein M is a metal, preferably Mg, and An- is an organic or inorganic anion. The pharmaceutically acceptable salts of such complexes also fall within the scope of the invention.
US8404681 Xanthones, thioxanthones and acridinones as DNA-PK inhibitors Compound that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods of inhibiting the DNA-PK biological activity, methods of sensitizing cells the agents that cause DNA lesions, and methods of potentiating cancer treatment are disclosed.
WO2007139984A2 Duloxetine hcl polymorphs A crystalline form of duloxetine hydrochloride, pharmaceutical compositions of the crystalline form of duloxetine hydrochloride, and methods of preparing the crystalline form of duloxetine hydrochloride are provided.
CN101961315B Ornithine aspartate liposome injection The invention discloses an ornithine aspartate liposome injection. The injection mainly comprises the following active ingredients: ornithine aspartate, dipalmitoyl phosphatidyl glycerol, cholesterol and antioxidant in part by weight of 1:3-20:1.8-12:0.05-0.2. The stability of the ornithine aspartate is improved; the valid period is prolonged; and the quality of the product is guaranteed. Becausethe liposome carriers, namely the dipalmitoyl phosphatidyl glycerol and the cholesterol, are degradable in bodies, the bioavailability is improved and the toxic and side effects are reduced. The injection has the advantages of simple production process, easy operation, low cost, high yield and suitability for mass production.
US20130022681 Granules for pharmaceutical preparations, methods and apparatus for their production Disclosed are improved granular pharmaceutical preparations, together with improved methods and apparatus for preparation of granules for use in such preparations. Such methods are especially useful for making granules for solid oral dose pharmaceutical preparations, and are particularly suited to the production of granules comprising 5-aminosalicylic acid (5-ASA) for the treatment of inflammatory bowel disease. The granules exhibit a more sharply peaked length distribution, and hence aspect ratio distribution, and have a consequently much sharper dissolution profile after further processing.
US20090312251 Methods of regulating differentiation in mammals Mechanisms regulating cell proliferation stop and differentiation initiation during the development stage of mammalian embryo, and the proteins involved therein, are presented. Differentiation regulators, methods of regulating differentiation, transgenic organisms with loss of expression of the differentiation regulator, and methods of preparing the transgenic organisms, are provided.
CN102871999A Application of 10-monoalkoxy taxad compound derivatives to preparation of antineoplastic drugs The invention discloses an application of 10-monoalkoxy taxad compound derivatives to preparation of antineoplastic drugs. The application belongs to the field of a medical technology, wherein the 10-monoalkoxy taxad compound derivatives are represented by a general formula (I). A study finds that compounds represented by the general formula (I) have obvious bioactivities in vitro and in vivo, particularly have activities on tumors capable of tolerating either taxol or docetaxel. The invention also discloses a medicinal composition containing amount of at least one compound represented by the general formula (I) for treating either human beings or domestic animals. The composition can be prepared by one or more of a medicinal cosolvent, a carrier or an excipient according to a conventional method.
CN1915233A Medicine composition for treating anxiety neurosis, and oral cavity disintegration preparation A composite medicine in the form particle or oral disintegrating tablet for enxiety is prepared from tandopsirone or its derivative and the pharmacologically acceptable additive. Its oral disintegrating form is also disclosed.
US7972777 Nucleic acid probe-based diagnostic assays targeting ssrA genes of prokaryotic and eukaryotic organisms Use of the ssrA gene or tmRNA, an RNA transcript of the ssrA gene, or fragments thereof as target regions in a nucleic acid probe assay for the detection and identification of prokaryotic and/or eukaryotic organisms is described. Nucleotide sequence alignment of tmRNA sequences from various organisms can be used to identify regions of homology and non-homology within the sequences which in turn can be used to design both genus specific and species specific oligonucleotide probes. These newly identified regions of homology and non-homology provide the basis of identifying and detecting organisms at the molecular level. Oligonucleotide probes identified in this way can be used to detect tmRNA in samples thereby giving an indication of the viability of non-viral organisms present in various sample types.
US20100112064 Transdermal therapeutic system comprising ion pair microreservoirs The invention relates to a transdermal therapeutic system which comprises a back layer that is impermeable to the active substance, and a peelable protective layer that is impermeable to the active substance and at least one matrix layer consisting of polysiloxanes and/or polysiloxane derivatives and containing micro-reservoirs. Said micro-reservoirs contain at least one ion pair from a pharmacologically active substance and an additive and either the active substance is nucleophilic and the additive is electrophilic or the active substance is electrophilic and the additive is nucleophilic.
EP1300395B1 4-substituted piperidine compound A novel compound having excellent acetyl cholinesterase inhibitory activity. It is a compound represented by the formula (I), a salt thereof, or a hydrate of these in said formula (I), R1 represents a group represented by the formula (a) wherein R?3, R4, R5, and R6¿ are the same or different and each represents hydrogen, optionally substituted C¿1-6? alkoxy, etc.; and m is an integer of 0 to 6, etc.; and R?2¿ represents hydrogen, optionally substituted C¿1-6? alkyl, optionally substituted C2-6 alkenyl, or optionally substituted C2-6 alkynyl.
US20090018197 Methods for treating status epilepticus and related conditions The present invention is directed to the novel use of a class of peptide compounds for treating status epilepticus or related conditions, e.g. acute repetitive seizures, seizure clusters, etc.
CN103127068A Application of Eryngiolide A in medicines promoting insulin secretion The invention belongs to the pharmacy field and discloses application of Eryngiolide A in medicines promoting insulin secretion. Use of the Eryngiolide A in preparation of medicines promoting insulin secretion is made public for the first time, the skeleton type is completely novel, and the Eryngiolide A has an unexpectedly high promoting insulin secretion activity, probability of other compounds giving any revelation for the Eryngiolide A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in preventing and curing type 2 diabet.
US20110064817 Continuous multi-microencapsulation process for improving the stability and storage life of biologically active ingredients The invention relates to microcapsules, and a continuous micro-encapsulation water-in-oil-in-water microencapsulation process through in situ and interfacial polymerization of the emulsion. The formulation comprises a continuous water phase having a dispersion of microcapsules which contain oil drops and wherein the inside of each oil phase drop—containing optionally oil-soluble materials—there is a dispersion of water, or aqueous extract or water dispersible material or water soluble material. The oil drops are encapsulated with a polymerisable material of natural origin. Such microcapsules are appropriated for spray-dry processes, to be used as dry powder, lyophilised, self-emulsifiable powder, gel, cream and any liquid form. The active compounds included in the microcapsules are beneficial to the health and other biological purposes. Such formulations are appropriate to be incorporated in any class of food, especially for the production of nutraceuticals, as well as cosmetic products (such as rejuvenescence creams, anti-wrinkle creams, gels, bath and shower consumable products and sprays). The preparations are adequate to stabilise compounds added to the food, media for cultivating microbes and nutraceuticals, especially those which are easily degradable or oxidizable.
WO2013101949A2 Composition and method for compounded therapy The present embodiments relate to topically delivered compounded medications. A transdermal cream may provide the effective topical administration of multiple medications simultaneously. The transdermal cream may include low concentrations of local anesthetics, a NSAID, an anticonvulsant, and/or other active ingredients. The transdermal cream may include lidocaine, prilocaine, meloxicam, and lamotrigine and/or topiramate. Alternatively, the transdermal cream may include a lidocaine/prilocaine base cream to which is added a fine powder of one or more ground up medications to form a compounded medication. The compounded medication in powder form may be generated from grinding up tablets of NSAIDs, anticonvulsants, nerve depressants, antidepressants, muscle relaxants, NMDA receptor antagonists, opiate or opioid agonists, and/or other agents. The compounded medication in powder form may include meloxicam, lamotrigine, topiramate, other active ingredients, and DMSO or Sterile Water for Irrigation. In another aspect, the present embodiments relate to methods of compounding medications and transdermal creams or gels.
WO2011066864A1 Method and compositions for inhibition of macrophage migration inhibitory factor (mif) The present invention relates to methods for inhibition of tautomerase activity of macrophage migration inhibitory factor (MIF). The invention further relates to substances for irreversibly covalently binding to MIF for inhibition of tautomerase activity.
WO2005023240A3 Pharmaceutical combination preparation containing glycyrrhizine, zinc, and a compound comprising a thiol group or a group that is metabolized thereto The invention relates to a combined pharmaceutical or nutritional supplement preparation containing glycyrrhizine, zinc, and a compound that is acceptable for oral administration and comprises at least one free thiol group or a group which is metabolized into a free thiol group in the body of a mammal. The inventive preparation is useful for fighting viral diseases, particularly influenza-type diseases.
US20100311809 Viral vector system, a composition comprising the viral vector system and its use The present invention relates to a viral vector system comprising at least one viral vector and at least one regulable expression cassette inserted in said viral vector applicable for the treatment of virally infected cells. Preferably, the at least one regulable expression cassette comprises at least one transactivator, at least one promoter and at least one nucleotide sequence coding for a transgene, preferably a fusion protein. The present invention also relates to a composition comprising said viral vector and antiviral siRNAs for treatment of virally infected cells.
US7138404 Anxiolytic agents and analgesics This invention is 4-aminopyrimidine derivatives of the formula wherein R1, R2, R3 and R4 are as defined in the specification or a pharmaceutically acceptable salt thereof. The invention also is the preparation of compounds of formula I, pharmaceutical compositions containing therapeutically effective amounts of compounds of formula I or pharmaceutically acceptable salts thereof and to a method of treatment comprising administering therapeutically effective amounts of the compound of formula I for the prevention or treatment of mGluR5 receptor mediated disorders.
US20080269350 St104p, an anti-angiogenic agent The present invention relates to a method of treating a non-tumor condition or disease associated with angiogenesis in a human or animal comprises administering thereto an effective angiogenesis inhibiting dose of a tetrameric cyclic compound of 4,5-dihydroxynaphthalene-2,7, disulfonic acid linked by methylene bridges in a pharmaceutically acceptable carrier.
US7071233 Microbe inhibitors comprising antimicrobial isolates, botanical extracts or phytochemicals; also Commiphora myrrha, Commiphora molmol, Commiphora erythraea, sequiterpenes, nutrient, a vitamin, or a vitamin B complex. An improved medical treatment and medicine is provided to quickly and safely resolve HIV and other microbial infections. The inexpensive medicine can be self administered and maintained for the prescribed time. The attractive medicine comprises an antimicrobial concentrate comprising microbe inhibitors, phytochemicals or isolates. Desirably, the effective medicine comprises a surfactant and an aqueous carrier or solvent and a nutrient. In the preferred form, the medicine comprises: Echinacea and Commiphora myrrha phytochemicals, benzalkonium chloride, a sterile water solution, and folic acid.
US7220779 Using 5-aminolevulinic acid A pig growth enhancer, which comprises, as an active ingredient, at least one compound selected from 5-aminolevulinic acid, a derivative thereof and a salt thereof, and a method for enhancing pig growth, which comprises administering the growth enhancer to a pig.
CN103396386A Di-substituted dinaphtho-[2,1-b:1',2'-d] furan derivative as well as preparation method and application thereof The invention relates to a di-substituted dinaphtho-[2,1-b:1',2'-d] furan derivative as well as a preparation method and an application thereof. The preparation method comprises the following steps of: synthesizing a series of di-substituted dinaphtho-[2,1-b:1',2'-d] furan derivatives through a series of reactions by using dibromo-dinaphtho-[2,1-b:1',2'-d] furan as the material. The invention further provides an application of the di-substituted dinaphtho-[2,1-b:1',2'-d] furan derivative in preparing an anti-tumor drug. By virtue of in-vitro pharmacological activity screening, the compound which is synthesized by the preparation method disclosed by the invention is shown to have an effect for inhibiting proliferation of tumor cells, wherein the compound 16 has an obvious inhibiting effect for the liver cancer cells SMMC-7721; and the IC50 value reaches 0.57mu M. Besides, the di-substituted dinaphtho-[2,1-b:1',2'-d] furan derivative is reasonable in design, simple and convenient in preparation method and strong in practicability.
WO2007109547A3 Method of preventing and treating hepatic disease using a2b adenosine receptor antagonists The invention is related to methods of preventing and treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment and prevention of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases. The invention also relates to pharmaceutical compositions for use in the method.
US20110213039 Infant formulas containing docosahexaenoic acid and lutein Disclosed is a method of reducing the risk or severity of retinopathy of prematurity in preterm infants. The method comprises (a) measuring skin carotenoid levels in preterm infants, preferably by Raman Spectroscopy, and then (b) administering supplemental carotenoids to those infants in need thereof, wherein the supplemental carotenoids comprise lutein, lycopene, beta-carotene, and zeaxanthin. The supplemental carotenoids may be provided by an infant formula comprising, on a ready-to-feed basis, from about 100 to about 2000 mcg/liter of total carotenoids, wherein the total carotenoids include at least about 50 mcg/liter of lutein. The formulas may further comprise docosahexaenoic acid.
US20090041858 Haemostatic Compositions Thickened by Polymers Containing Nitrogen Moieties The present invention is the development of haemostatic compositions that use nitrogen containing organic polymers in combination with haemostatic agents to create a gel form. Compositions utilizing the polymers exhibit relatively lower concentrations of haemostatic agents, drawing benefits from such lower concentrations as they limit unwanted side effects of the haemostatic agents. Preferred compositions utilize Poly(N-vinylpyrrolidone), Poly(2-ethyl-2-oxazoline) as thickening agents and ferric sulfate as an active ingredient.
US20080267873 Aqueous injection buffer containing sodium chloride, calcium chloride, potassium chloride in the preparation of a RNA injection solution for increasing RNA transfer, RNA translation in a host organism The invention relates to the use of RNA and an aqueous injection buffer containing a sodium salt, a calcium salt and optionally a potassium salt and optionally lactate, in the preparation of a RNA injection solution for increasing RNA transfer and/or RNA translation into/in a host organism. The invention relates further to a RNA injection solution and to a method for increasing the RNA transfer and/or RNA translation of RNA in vivo and in vitro.
EP1982707A1 Use of hydroxytyrosol as anti-aging agent The present invention is directed to the use of (a composition comprising) hydroxytyrosol as anti-aging agent. The composition, to which the present invention is also directed, does essentially not comprise resveratrol and is administered orally to animals. The present invention is further directed to anti-aging methods. "Anti-aging" meaning in the context of the present invention: retarding the aging processes in said animals, improving age-related physiological deficits in said animals and/or promoting a healthy aging in said animals.
CA2152973C Phosphinic acid derivatives, their preparation and their use Compounds of the formula I, (see formula I) in which the symbols or substituents A, B, D, D*, E and E* have the specified meanings, inhibit aspartyl proteases and are suitable for controlling viral diseases.
CN103588861A New Delhi metallo-beta-lactamase inhibitory peptide and application thereof The invention belongs to the field of biological medicament, and specifically relates to a NDM-1 type metallo-beta-lactamase tripeptide inhibitor with an amino acid sequence of Phe-Cys-D-Phe. Pharmacodynamical experiments prove that the peptide provided by the invention is applicable to preparation of antibacterial medicaments for preventing and treating drug-resistance bacterial infection.
CN103341029A Cordyceps wind-dispelling detoxifying powder and preparation method thereof The invention relates to an external-treatment Tibetan drug and a preparation method thereof, and in particular relates to cordyceps wind-dispelling detoxifying powder which penetrates through skin to reach a human acupuncture point or focus by virtue of drug gas and a preparation method of the powder. The formula of cordyceps wind-dispelling detoxifying powder comprises the following components in parts by weight: 1-2 parts of cordyceps, 1-2 parts of typhonium giganteum, 1-2 parts of lilies, 1-2 parts of saffron crocus, 1-2 parts of rhodiola rosea, 1-2 parts of leeches, 1-2 parts of venenum bufonis, 1-2 parts of radix pseudostellariae, 1-2 parts of ginkgo seeds, 1-3 parts of monkshood and 1-3 parts of musk, wherein the weight of sulfur is 1.5 times of the weight of the 12 drugs. The pharmaceutical formula and pharmaceutical preparation technology of the cordyceps wind-dispelling detoxifying powder sufficiently utilize natural properties of the drugs, for example liquid properties and combustion properties of the sulfur. The disease-treatment gas formed by the drug combustion penetrates into the skin to directly reach the human inner acupuncture point or focus to achieve the purpose of treating the disease.
EP1259231B1 Naphthoquinone derivatives as cd45 inhibitors Substituted naphthalenediones in accord with structural diagram (I): compositions thereof and methods for the use thereof, for the treatment of T cell mediated conditions such as autoimmune diseases and organ graft rejection. In compounds of the invention, wherein: Q1 at each occurrence is independently selected from hydrogen, hydroxy, halogen, C(O)O(C¿1?-C3) alkyl and C(O)phenyl, and Q?2¿ is selected from hydrogen, halogen, O-(C¿1?-C3)alkyl, O-(C1-C3)alkenyl, phenyl, indolyl and naphthyl, where phenyl may be mono- or di-substituted with NO2 or halogen, and indolyl may be substituted with (C1-C3)alkyl or phenyl.
CN101018846B Method for producing unsaturated fatty acid concentrate An easy and inexpensive process by which a concentrate of a given unsaturated fatty acid can be obtained from a mixture which has conventionally been difficult to concentrate. The process, which is for producing a concentrate of a desired isomer (a) from a mixture (A) selected from the group consisting of a mixture comprising at least two isomers of a C16 or higher conjugated unsaturated fatty acid and a mixture comprising at least two cis-isomers of a C16 or higher unsaturated fatty acid having a cis-double bond, is characterized by comprising: a step in which the mixture (A) is mixed with atleast one C4-14 saturated fatty acid (B) to obtain a mixture solution containing the isomer (a) dissolved therein; a crystallization step in which either crystals rich in the isomer (a) or crystals poor in the isomer (a) are precipitated from the mixture solution; and a solid-liquid separation step for obtaining the crystals rich in the isomer (a) or for obtaining a solution rich in the isomer (a)by removing the crystals poor in the isomer (a).
US20120316066 Chiral Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.
CN103110584A Tiotropium bromide powder inhalation and preparation method thereof The invention discloses a tiotropium bromide powder inhalation, which is obtained by carrying out micro powder treatment on a tiotropium bromide raw material, separating the raw material with the grain size in a range of 1-5 microns through a multistage cascade impactor NGI, mixing with inhalable lactose, and encapsulating. The grain size of the tiotropium bromide raw material of the tiotropium bromide powder inhalation provided by the invention is in the range of 1-5 microns, so that the security and the effectiveness in drug use can be improved.
CN103664867A Acylhydrazone derivatives containing 1,4-benzodioxane, and preparation method and antibacterial activity thereof The invention discloses acylhydrazone derivatives containing 1,4-benzodioxane, of which the general formula is disclosed in the specification, wherein R is disclosed in the specification. The acylhydrazone derivatives containing 1,4-benzodioxane have different inhibiting actions on B. subtilis, S. aureus, E. coli and P. aeruginosa, and thus, can be used in preparing antibacterial drugs. The invention also discloses a preparation method of the acylhydrazone derivatives containing 1,4-benzodioxane.
EP1547579A1 Adhesive gel composition for iontophoresis preparation and process for producing the same The present invention provides an adhesive gel composition for iontophoretic formulations which is useful for the application through the skin or the mucosa, which excels in all of drug absorption, drug stability, gel shape retention and gel adhesion, which is easy to prepare and fill at the time of production, and which can be produced at low costs and a method for producing the same. The adhesive gel composition for iontophoretic formulations is produced by mixing an ionic synthetic polymer(s), a nonionic synthetic polymer(s), a naturally-occurring polymer(s), a polyhydric alcohol(s), a crosslinking agent(s) and a drug(s). In the production of the adhesive gel composition for iontophoretic formulations, oxygen dissolved in the gel is positively removed by carrying out replacement with nitrogen and/or vacuum kneading at the time of the ingredients are mixed and kneaded.
CN102351823A Lactucin derivative, and preparation method and application thereof The invention relates to a lactucin derivative, and a preparation method and application thereof. The lactucin derivative is synthesized by performing structural modification on lactucin which is separated from Cichorium glandulosum Boiss. et Huet and is taken as a parent compound. The activity result of the derivative shows that: the derivative has better effects of inhibiting A549 human lung cancer cells, HL-60 human leukemia cells, Bel-7402 human liver cancer cells and KB human nasopharyngeal darcinoma cells; meanwhile, the derivative is independent or combined with one or more pharmaceutically acceptable, inert and nontoxic excipients or carriers to form a medicinal composition to be applied to the development of antitumor medicines.
CN101366716B Application of Raloxifene compounds in preparing medicament for preventing and controlling benign prostatahyperplasie The invention belongs to the medicinal field, and in particular discloses application of a raloxifene compound in preparing medicines for preventing and treating nonmalignant prostate hyperplasia. As verified by cell and animal model experiments, the raloxifene compound has obvious inhibition effect on proliferation of prostate interstitial cells, can resist the proliferation promoting effect of estradiol on the interstitial cells, and has obvious effect of treating and improving the pathologic change that estrogen/androgen induces prostate interstitial proliferation of an emasculated mouse.
US20130065904 Combinations of Eszopiclone and Trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-N-Methyl-1-Napthalenamine or Trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-1-Napthalenamine, and Methods of Treatment of Menopause and Mood, Anxiety, and Cognitive Disorders One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine or trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.
CN102216316A Substituted amine derivative and medicinal composition comprising same as the active ingredient A compound represented by general formula (I) [wherein --- represents a single bond or a double bond; L represents -NH- or the like; X1 represents N or C, provided that in the case where X1 is N, X2 represents C-R and in the case where X1 is C, X2 represents N-R1 or the like; Y's may be either the same or different and represent CH2 or the like; A represents a non-natural sugar residue represented by general formula (II) [wherein m represents 0 to 1; --- represents a single bond or a double bond; X represents 0 or the like; and R3 to R9 may be either the same or different and represent a hydroxyl group or the like]; and B represents a group represented by general formula (III) [wherein n and k represent 0 to 5; --- represents a single bond or a double bond; Z1 to Z16 may be either the same or different and represent CH or the like; R10 and R11 may be either the same or different and represent a lower alkoxy group having 1 to 5 carbon atoms or the like; and R15 represents a hydrogen atom or the like]], a pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate thereof or a solvate thereof. Because of having an excellent CNT2 inhibitory activity and showing a high in vivo stability and stable physicochemical properties, the aforesaid compound is useful as a remedy for hyperuricemia.
WO2007142286A1 Fatigue-reducing agent A pharmaceutical product, a functional food or the like has been demanded which can reduce the fatigue in a tired person and enables the tired person to lead a fulfilled life. Disclosed is a fatigue-reducing agent. The fatigue-reducing agent comprises ornithine or a salt thereof and glutathione or a salt thereof as active ingredients.
CN101683319B Tirapazamine parenteral hydrous preparation and preparation method thereof The invention provides a Tirapazamine parenteral hydrous preparation and a preparation method thereof. The preparation comprises the following basic components: a citrate buffer solution and Tirapazamine or available salts thereof, wherein the concentration of the buffer solution is 0.02-0.99 mmol/l, and the buffer solution is acceptable in medical preparations; the concentration of the Tirapazamine or available salts thereof is 0.056-0.091 mmol/l; and the pH value of the preparation is 3.0-6.5. The preparation solves the problem of easy precipitation when the solution of Tirapazamine is put still in the prior art, enhances the stability and the safety of the preparation and meets the clinical and broad patients' requirements for the preparation.
WO2010058669A1 Novel prostaglandin e1 derivative, and nanoparticle having same encapsulated therein The object is to provide a PGE1 derivative having excellent duration of action of PGE1 and excellent slow release properties, and to prepare nanoparticles of the PGE1 derivative to provide PGE1-derivative-containing nanoparticles which can target at an affected area efficiently, has excellent slow drug release properties, and has reduced adverse side effects. Disclosed is a prostaglandin E1 derivative represented by formula (I) [wherein n represents an integer of 1 to 12]. Also disclosed are nanoparticles containing the prostaglandin E1 derivative, which is produced by hydrophobizing the prostaglandin E1 derivative with a metal ion and reacting the resulting product with a poly (L-lactic acid) or a poly (L-lactic acid/glycolic acid) copolymer and a poly(DL- or L-lactic acid)-(polyethylene glycol) block copolymer or a poly (DL- or L-lactic acid/glycolic acid)-(polyethylene glycol) block copolymer.
CN101032471A Chuanhuning lipid freeze-dry powder agent and preparing method thereof The present invention relates to freeze dried liposome powder preparation containing Chuanhuning (andrographis paniculata) and its preparation process. The freeze dried liposome powder preparation has Chuanhuning as the effective component in 1 weight portions, phospholipid containing liposome in 1-200 weight portions, emulsifier in 0.0001-50 weight portions, freeze drying protectant and supplementary material in proper amount. The freeze dried liposome powder preparation containing Chuanhuning has high storage stability, high water solubility, packaging rate of 50-100 % and grain size of 40-1000 nm. The present invention may be prepared into injection, oral preparation and other pharmaceutically acceptable forms, and is suitable for industrial production.
EP1858877A1 1,3 substituted diaryl ureas as modulators of kinase activity Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof , are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Use in treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom
CN101693008A Ofloxacin injection and preparation process thereof The invention discloses an ofloxacin injection which is prepared by ofloxacin, acetic acid, disodium tetracemate, propylene glycol and water for injection. The invention solves the problem that an ofloxacin injection hydro-acupuncture is easy to crystallize through adopting the acetic acid as cosolvent and improving the dissolvability of ofloxacin by adding the propylene glycol to regulate the polarity of solution. The injection provided by the invention has excellent quality stability, solves the problem of crystallization commonly existed in products of ofloxacin injection hydro-acupuncture, solves the weaknesses of instability and short retention period of injection, reduces the number of insoluble particles in medicine solution, and provides the effective guarantee for the safe use in clinics.
CN1640404A Ganciclovir injection liquid and its production method The present invention relates to a ganciclovir injection and its production method. Said production method includes the following steps: 1. using proper quantity of injection water to dissolve active raw material ganciclovir; 2. mixing medicinal auxiliary material with ganciclovir aqueoue solution obtained by step 1. and making ganiclovir be completely dissolved; 3. regulating pH value of solution obtained by step 2. to 7.0-10.0, adding injection water to total dose; and 4 according to requirements of GMP and QC of drug producing ganciclovir injection.
US6852727 Inhibitors of Janus protein tyrosine kinases (Jak), and as such are useful as immunosuppressants, and in the treatment of diseases including asthma, allergies, autoimmune diseases. Benzimidazo[4,5-f]isoquinolinone derivatives are inhibitors of Janus protein tyrosine kinases (Jak), and as such are useful as immunosuppressants, and in the treatment of diseases including asthma, allergies, autoimmune diseases.
US8178713 Sulfur-containing phospholipid derivatives The present invention provides a lipid compound comprising at least one non-polar moiety and a polar moiety, wherein each or at least one non-polar moiety is of the formula X—Y—Z—, wherein X is a hydrocarbyl chain, Y is selected from at least one of S, Se, SO2, SO, and O, and Z is an optional hydrocarbyl group, wherein the polar moiety is of the formula —[C(O)]mPHG, wherein PHG is a polar head group, and wherein m is the number of non-polar moieties.
US8287888 Thermosensitive polyphosphazene-bioactive molecule conjugates, preparation method thereof and use thereof The present invention relates to a poly(organophosphazene)-bioactive molecule conjugates in which biodegradable and thermosensitive poly(organophosphazene) with a functional group showing the sol-gel phase transition with change of temperature is combined with various bioactive molecules, such as drugs, a preparation method thereof, and a use thereof for delivery of bioactive molecules.
US20080064752 Nonhygroscopic photosensitizing agents; sulphonate, hydrobromide, sulfate, nitrate and/or phosphate derivatives; diagnosing skin disorders The present invention provides an acid addition salt of 5-aminolevulinic acid (5-ALA) or of a 5-ALA derivative (e.g. a 5-ALA ester) with an acid which has a pKa of about 5 or less, preferably about 3 or less, with the proviso that the acid is other than hydrochloric acid. Particularly preferred salts are those derived from acids selected from the group comprising sulphonic acid and its derivatives, hydrobromic acid, sulfuric acid, nitric acid and phosphoric acid. The salts in accordance with the invention are particularly suitable for use as photosensitizing agents in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body.
US20090054511 S)-(+)-N-acetyl-2,4,6-tribromo-5-methoxytryptophan methyl ester (4) from (S)-(+)-N-acetyl-5-methoxytryptophan methyl ester; osteoporosis, osteoblast activator It is intended to provide a tryptophan derivative that activates osteoblasts and to provide a therapeutic drug for osteoporosis and an osteoblast activator using this tryptophan derivative. This invention relates to a compound represented by the following formula (I) or a salt thereof: wherein X represents a halogen atom; R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl group, substituted or unsubstituted C2-6 alkenyl group, substituted or unsubstituted C2-6 alkynyl group, substituted or unsubstituted aromatic group, substituted or unsubstituted aralkyl group, substituted or unsubstituted acyl group, substituted or unsubstituted arylsulfonyl group, substituted or unsubstituted C1-6 alkylsulfonyl group, substituted or unsubstituted C2-7 alkoxycarbonyl group, or hydroxyl group; R2 represents a substituted or unsubstituted C1-21 alkyl group; R3, R5, and R6 are the same or different and represent a hydrogen atom or halogen atom; R4 represents a hydrogen atom or substituted or unsubstituted C1-6 alkyl group; and R7 represents a hydrogen atom or substituted or unsubstituted C1-21 hydrocarbon group, and to a therapeutic drug for osteoporosis and an osteoblast activator comprising the compound or a salt thereof.
US20080221059 Novel treatment tool for cancer: rna interference of bcas2 The present invention provides three BCAS2 related nucleotide sequences. The present invention also provides a composition comprising a nucleotide sequence of small interfering RNA of BCAS2 gene. The present invention further provides a method for treating p53 containing cancer comprising administrating a subject with an effective amount of the said composition.
CN1615894A Notoginseng total saponin amino acid transfusion liquid and its producing method The present invention discloses total arasaponin-amino acid transfusion liquid, and features that each bottle of the transfusion liquid contains total arasaponin 0.10-1.00 g, amino acid for providing nutrients and energy, and medicinal supplementary material. It has stable quality, no irritation and high curative effect. It has double functions of promoting blood circulation to disperse blood clots and providing nutritive and supporting components. It is used in salvage of serious patient of cardiac and cerebral vascular diseases and special diseases.
WO2009051909A1 Compounds having activity in correcting mutant-cftr cellular processing and uses thereof The invention provides compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The compositions pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The compositions and pharmaceutical preparations of the invention may comprise one or more bithiazole-containing compounds of the invention, or an analog or derivative thereof.
CN101837083B Ointment for curing burns and scalds and preparation method thereof The invention relates to an ointment for curing burns and scalds, which is prepared from the following raw material medicaments: 10 to 50 parts of natural indigo, 1 to 10 parts of borneol, 1 to 10 parts of mint, 10 to 30 parts of golden thread, 10 to 50 parts of Chinese angelica, 10 to 30 parts of Chinese gall, 10 to 30 parts of campanumaea pilosula, and 5 to 20 parts of dragon's blood. The invention also relates to a preparation method of the ointment. The ointment has the advantages of direct administration on wound, simple operation, no need of cleaning wounds before administration, pain alleviation of patients, and effective treatment for the burns and scalds.
CN102838504A Novel agomelatine crystal form L and preparation method thereof The invention belongs to the technical field of pharmaceutical chemical synthesis and relates to a novel agomelatine crystal form L and a preparation method thereof. The preparation method of the novel Agomelatine crystal form L comprises the following steps of: adding an agomelatine crude product into a solvent and heating and dissolving the agomelatine crude product; then cooling to the room temperature, naturally volatilizing to be dry; and finally obtaining the product through vacuum drying.
US20100255088 Method for delivering a combination of resveratrol and aspirin for use in treatment and prevention of vascular disease A method for delivering a composition for use in treatment and prevention of vascular disease by providing a vehicle for delivery of the composition to an individual, wherein the composition contains a combination of aspirin and resveratrol; administering the vehicle to the mouth of the individual, wherein the vehicle melts at the body temperature of the individual such that the aspirin and resveratrol is absorbed thru the oral mucosa and delivered directly into the inidvidual's bloodstream; and a related melting capsule comprised of a material that has the same melting point as the human body temperature and includes aspirin in the range of 81 to 325 mg and resveratrol in the range of 10 to 300 mg.
US8569305 Treatment of tuberous sclerosis associated neoplasms The present invention relates to the use of PDGF receptor tyrosine kinase or bcr-abl tyrosine kinase inhibitors, especially of N-phenyl-2-pyrimidine-amine derivatives of formula I, in which the symbols and substituents have the meaning as defined herein in free form or in pharmaceutically acceptable salt form, in the manufacture of a pharmaceutical composition for the treatment of tuberous sclerosis associated neoplasms; to a method of treatment of warm-blooded animals, including humans, suffering from a tuberous sclerosis associated neoplasms.
US20120015993 Novel Pharmaceutical Forms, and Methods of Making and Using the Same Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided.
CN1869051A Preparation method of trialcohol group ginseng saponine and dialcohol group ginseng saponine A process for preparing triol group and biol group of ginsenosides includes such steps as preparing the extract from ginseng or red ginseng, adsorbing with macroreticular resin, eluting with low-concentration organic solvent, recovering solvent to obtain triol group of ginsenosides, eluting with high-concentration organic solvent, and recovering solvent to obtain biol group of ginsenosides.
WO2013133723A1 Synthesis of elemicin and topical analgesic compositions The present invention is directed to the synthesis of elemicin and its isomeric form, and their use in topical analgesic formulations, including for dental and veterinary use. Various compositions include gels, films, dressings, cavity filling gels, having analgesic and/or antifungal properties.
EP0927036B1 Transdermal therapeutical approach involving a combination of bisphosphate containing oestriol Disclosed is a transdermal therapeutical approach involving oestriol as an active substance, characterized in that oestriol is combined with one or more active substances.
EP2044958A2 Pharmaceutical composition for treating arteriosclerosis A pharmaceutical composition comprising a group V or X sPLA2-inhibiting compound represented by general formula (I) : wherein ring A is: -B- is a group of (e)-(h): for use in suppressing degeneration of serum lipoproteins and/or treating or preventing arteriosclerosis and/or treating or preventing an ischemic disease based on arteriosclerosis.
EP1017680B1 Tricyclic compounds, preparation method and said method intermediates, application as medicines and pharmaceutical compositions containing same The invention concerns products of formula (I) in which R1 represents -CONH - [A] - [B] -COR6, [A], [B]; R2, R3, R4, R5 and G are as defined in the description, and their salt additives with acids, bases and esters, the method for preparing them and the intermediates of said method, their application as medicines and the pharmaceutical compositions containing them.
CN101332302A Formula for preparing anti-eczema and cutitis products and preparation method thereof The invention relates to a formula for preparing an anti-eczema dermatitis product and the preparation method thereof. The invention adopts dexamethasone, menthol, phenol and boric acid compatibly for external use for the first time and provides an anti-eczema dermatitis product which also has multiple prevention functions of anti-allergy, anti-pruritus, anti-infection, and the like; the formula has the advantages of remarkable and quick antipruritic effect, strong bacteriostasis, small toxic side effect, and positive curative effect; ideal effect can be achieved when the anti-eczema dermatitis product is in direct use; more particularly, the tincture formula thereof has the advantages of stable property, simple preparation technology, safety and effectiveness, good feasibility, high repeatability, and controlled quality, and is suitable for the industrial production. The eczema dermatitis has diverse categories and etiologies, complicated disease diagnosis, and very high incidence and relapse rate; the anti-eczema dermatitis product of the invention has a plurality of usages, can enhance medical effect, is convenient to select in clinic, and can reduce the economic burden of the patients; therefore, with the number of dermatitis patients increasing year by year, the demand for therapeutic medication can be also increased; the formula and the preparation method thereof can produce greater social and economic benefits.
US20110182964 Vascular Stent Which Elutes Amino Acid-Methyl-Ester Derivatives for the Treatment of Vulnerable Plaque and Vascular Disease This invention provides implantable medical devices that include delivery systems containing amino acid derivatives, and related methods for making and using. More specifically, this invention provides vascular stents with coatings containing methyl ester derivatives of amino acids, and related methods for making and using.
US20060235026 Quinoline-4-Carboxamide Derivatives as NK-3 and NK-2 Receptor Antagonists Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: wherein: R1 is H or C1-6 alkyl; R2 is aryl or C3-7 cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is R8R9; R8 is a single bond, C1-6 alkyl, or aryl; R9 is H, COO R10, or NR11R12; R10 is H or C1-6 alkyl; R11 and R12 are independently selected from H and C1-6 alkyl; R5 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, aryl, or a single or fused ring aromatic heterocyclic group; R6 represents H or up to three substituents independently selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- or di-C1-6 alkylamino; R7 is H or halo; a is 1-6; and any of R2, R5, R8, R10, R11 and R12 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy or oxo; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.
CN103316014A Specific acupuncture function composite material, preparation method thereof and applications The invention relates to a specific acupuncture function composite material, which is composited from 3-30% of tourmalinite, 0.1-10% of mediation reinforcement dosage, 5-30% of mediation active medicament raw material, 30-60% of high-molecular material, and 0.5-5% of coupling agent. The specific acupuncture function composite material can be used for clinic medical health care, can be used as a channel and point treatment tool, and can be used for rehabilitation and treatment of relative diseases.
CN1772295A Application of cysteamine and its derivative in preparing medicine for raising potency of vaccine antibody The present invention provides new use of cysteamine and its derivative, and is especially the application of cysteamine and its derivative in preparing medicine for raising the antibody potency of human or veterinary vaccine, the immune response reaction and the disease resistance of body. Cysteamine or its derivative is used alone or prepared into medicine composition. The composition may be added into medicine for human or feed for animal to obtain medicine for human or feed for animal with cysteamine. Or, cysteamine or its derivative may be dissolved in water alone or together with stabilizer or metabolism reinforcing agent to prepare injection to be injected to human body or animal body directly or after being emulsified together with mineral oil before or during injecting vaccine.
US20090092668 Acetaminophen formulation for joint pain relief The invention relates generally to a formulation which may comprise additional vitamins, minerals, herbs and supplements and methods for using the same for joint pain relief. The formulation may comprise supplements such as glucosamine, hyaluronic acid and methylsulfonylmethane (MSM) and acetaminophen for acute joint pain. The invention also encompasses methods for joint pain relief with the formulation described herein.
US7649000 (2'S,2''R)-4-(2'-(2''-amino-3''-(4'''-ethoxyphenyl)propanoylamino)-3'-phenylpropanoyl-amino)piperidine- 1-carboxamidine; inflammatory bowel disease, arthritis, inflammation, septic shock, hypotension, cancer, adult respiratory distress syndrome, disseminated intravascular coagulation Compounds of general formula 1, or a pharmaceutically acceptable salt thereof, wherein R1 is selected from H, lower alkyl, R4—CO, R4—O2CCH2, R5—OCO and R5—SO2; R2 is selected from lower alkyl, cycloalkyl optionally substituted with an alkyl or alkyloxy group, (C5-C12)cycloalkylalkyl optionally substituted with an alkyl or alkyloxy group, aralkyl optionally substituted with up to three groups chosen from F, Cl, Br, I, OH, lower alkyl, O-(lower alkyl), O-benzyl, NH2, NO2, NH-acyl, CN and CF3, and aralkyloxymethyl optionally substituted with up to three groups chosen from F, Cl, Br, OH, lower alkyl and O-(lower alkyl); or R1 and R2 together are an o-xylylene group optionally substituted on the aromatic ring with a group selected from F, Cl, Br, OH, lower alkyl and O-(lower alkyl); R3 is selected from H, OH and O-lower alkyl; R4 is selected from H, lower alkyl and phenyl; and R5 is selected from lower alkyl, phenyl and benzyl. The compounds are useful as pharmaceutical compositions.
CN101919867A Method for constructing animal model of Mesocricitus auratus suffering from pancreatic cancer for nuclear magnetic resonance research The invention relates to a method for constructing an animal model of Mesocricitus auratus suffering from pancreatic cancer for nuclear magnetic resonance research. The used animal is Mesocricitus auratus, the used carcinogenic inducing substance is N-nitroso dual (2-propylene oxide) amine. The construction method comprises the following steps: preparing the carcinogenic inducing substance, namely the N-nitroso dual (2-propylene oxide) amine into carcinogenic inducing liquid with a concentration of 1mg/ml with normal saline; calculating each injection dosage of carcinogenic inducing liquid according to the standard that 10mg of N-nitroso dual (2-propylene oxide) amine is injected for per kilo of the weight of the Mesocricitus auratus at a time; carrying out subcutaneous injection on the back of the Mesocricitus auratus according to the calculated dosage of the carcinogenic inducing liquid for 7 weeks in a row and at a frequency of once a week; and keeping the Mesocricitus auratus normally for at least 23 weeks when the injection is stopped, thus forming the animal model of the Mesocricitus auratus suffering from pancreatic cancer.
US20070287703 Fused Pyrimidones Useful in the Treatment and the Prevention of Cancer Compounds which possess Eg5 inhibitory activity and are useful for their anti-cell-proliferation (such as anti-cancer) activity and thus in methods of treatment of the human or animal body are described.
CN103417528A New application of isojacareubin The invention discloses a new application of isojacareubin. The new application is meant that isojacareubin as an active ingredient is used in preparation of an antitumor pharmaceutical preparation. Pharmacological tests prove that, isojacareubin has an obvious inhibition effect on growth of U87 human brain glioma cell lines, BXPC-3 human pancreatic cancer cell lines, NCI-2126 human lung cancer cell lines, PANC-1 human pancreatic cancer cell lines, A549 human non small cell lung cancer cell lines, AGs human gastric cancer cell lines, A375 human melanoma cell lines, MCF-7 human breast cancer cell lines, MDA-MB-231 human breast cancer cell lines and SMMC-7721 human liver cancer cell lines, has significant antitumor activity, can be expected to be used as the active ingredient for the preparation of the antitumor pharmaceutical preparation, and has medicinal prospects.
CN101134108A Desonide cyclodextrin clathrate compound and method for preparing the same The present invention relates to cyclodextrin inclusion compound of desonide and its preparation process. The cyclodextrin inclusion compound of desonide has molecule ratio between desonide and cyclodextrin of 0.1-2. It is prepared through adding the alcohol solution of desonide into the water solution of cyclodextrin to include. Compared with common desonide preparation, the cyclodextrin included desonide preparation has obviously raised stability.
US20050058647 Newly identified polypeptide and polynucleotides for diagnosis of new compounds This invention relates to newly identified polypeptides and polynucleotides encoding such polypeptides sometimes hereinafter referred to as “novel phosphodiesterase type 7b (PDE7b)”, to their use in diagnostic and in identifying compounds that may be agonists, antagonists that are potentially useful in therapy, and to production of such polypeptides and polynucleotides.
CA2243235C Immunotherapy using cytotoxic t lymphocytes (ctl) A method of treating a patient with a disease wherein the patient contains diseased cells which cells contain, or are associated with, an abnormal molecule or an abnormally elevated amount of a molecule and which cells are capable of presenting at least part of said molecule on their surface by an HLA class I (or equivalent) molecule, the method comprising administering to the patient a therapeutically effective amount of cytotoxic T lymphocytes (CTL) which recognise at least part of said molecule when presented by an HLA class I (or equivalent) molecule on the surface of a cell characterised in that the cytotoxic T lymphocytes are not derived from the patient with a disease. Preferably, the CTL are derived from an individual which individual does not carry the HLA class I (or equivalent) molecule type which, in the patient, presents at least part of said abnormal molecule, or molecule abnormally elevated, contained in or associated with the disease cells of said patient.
WO2013108644A1 Rebamipide therapeutic agent for allergic conjunctivitis The present invention relates to an allergic conjunctivitis therapeutic agent having rebamipide or a pharmaceutically acceptable salt thereof as an active constituent.
WO2011022348A1 Ethylene diamine modulators of fatty acid amide hydrolase Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.
EP1495031A1 Labeled oxazinocarbazoles as diagnostic agents The present invention provides isotopically labeled oxazinocarbazole derivatives having a ring connecting position 8 (C-8) and position 9 (N-9), and more specifically, provides compounds of formula (I) wherein R1, R2, R3 and R4 are described herein. These compounds are useful in the diagnostic analysis of diseases wherein modulation of 5-HT activity is desired.
EP1035842B1 IMPROVED HMG CoA REDUCTASE INHIBITOR EXTENDED RELEASE FORMULATION A controlled release dosage formulation is described which is based on a combination of: (a) a compressed tablet core which contains an alkyl ester of a hydroxy substituted naphthalene derivative, a pharmaceutically acceptable, water swellable polymer and an osmotic agent; and (b) an outer coating layer which completely covers the osmotic core and comprises a pH sensitive coating agent and a water insoluble polymer.
WO2009013433A3 Use of pactimibe for the preparation of a drug intended to prevent or treat a disease caused by a sebaceous gland dysfunction in humans or animals The invention relates to the use of at least one compound selected from among N-(1-octyl-5-carboxymethyl-4,6-dimethylindolin-7-yl)-2,2-dimethylpropanamide (pactimibe) having formula (I), the pharmaceutically acceptable salts thereof and the pharmaceutically acceptable solvates of same, for the preparation of a drug intended to prevent or treat a disorder caused by a sebaceous gland dysfunction in humans or animals, such as acne and/or any condition or disorder linked to an overproduction of sebum, for example seborrheic dermatitis, oily skin or oily scalp.
EP1094804B1 The treatment of renal colic with gaba analogs The instant invention is a method of using certain analogs of glutamic acid and gamma-aminobutyric acid to relieve the pain associated with renal colic.
CA2218619C Antibacterial-wound healing compositions and methods for preparing and using same This invention pertains to therapeutic antibacterial-wound healing compositions. The compositions comprise a therapeutically effective amount of an antibacterial agent and a wound healing composition. In one embodiment the wound healing composition comprises (a) pyruvate; (b) an antioxidant; and (c) a mixture of saturated and unsaturated fatty acids. The therapeutic antibacterial-wound healing compositions may be utilized in a wide variety of pharmaceutical products. This invention also relates to methods for preparing and using the therapeutic antibacterial-wound healing compositions and the pharmaceutical products in which the therapeutic compositions may be used.
US20100034835 Use of inhibitors of leukotriene b4 receptor blt2 for treating asthma The present invention relates to a new use of inhibitors of leukotriene B4 receptor BLT2 for treating asthma. More particularly, the present invention relates to a pharmaceutical composition for treating asthma comprising BLT2 inhibitors and a method for treating asthma using BLT2 inhibitors. The present inventors investigated the role of BLT2 in the pathogenesis of asthma using a murine model and demonstrated that BLT2 plays a critical role in the development of AHR and airway inflammation by employing BLT2 inhibitors, such as antisense oligonucleotide. Therefore, the BLT 2 inhibitors according to the present invention can be effectively used as a therapeutic composition for treating asthma.
EP1930002A1 Use of hydroxybenzoic acid ester and analogues for the manufacture of a mendicament for the prevention and treatment of virus infection The use of hydroxybenzoic acid ester and analogues for the manufacture of a medicament for the prevention and treatment of viruses infection, especially human and animal HBV, HPV and HSVinfection is provided, wherein virus infection comprises HB, herpes simplex, condyloma acuminatum, vaginitis, cervicitis, and cervical erosion. Otherwise, the various kind of medicament and personal nursing product which are prepared by hydroxybenzoic acid ester and analogues and pharmaceutical adjuvant are provided.
EP1919463B9 Use of hif 1alfa modulators for treatment of cancer The invention relates to methods and compounds for treating or preventing cancer. Methods for treating or preventing cancer, for inhibiting tumor growth, reducing tumor volume, inhibiting tumor progression, inhibiting metastasis, and improving survival are provided herein.
CN1714871A Use of human ING4 gene as chemotherapy medicine sensitivity promoter The present invention discloses the use of human inhibitor of growth 4 (ING4) gene as tumor treating chemotherapy medicine sensitizer. The present invention also discloses one method of raising the sensitivity of tumor cell on chemotherapy medicine, and the method includes introducing ING4 gene into tumor cell before chemotherapy. Therefore, ING4 gene may be applied in the tumor treating chemotherapeutic process to promote the sensitivity of tumor cell on chemotherapy medicine, so as to reduce the dosage of chemotherapy medicine and reduce the toxic side effect of chemotherapy medicine on health cell of body.
WO2010115869A1 Propofol phosphonyl derivatives, synthesis, and use in long acting formulations This invention relates to compounds represented by the structural formula (I), and the salts and stereoisomers thereof, wherein: - L is a linker selected from the group consisting of -(CH2)P-O-, a single bond, formula (IA), -(CH2)1-8-O-X(O)-, and - p is an integer from 1 to 8, - each R3 and each R4 is independently selected from the group consisting of C1-20alkyl, C3-12alkyl, C3-12cycloalkyl-C1-4alkyl, saturated heterocyclyl and saturated heterocyclyl-C1-4alkyl, and - X and Y are each independently C or S(O), - Z is selected from the group consisting of O, S(O) and NR5, - W is selected from the group consisting of halogen, OH, S(O)H and O-M+ wherein M+ is a monovalent cation; and - R5 is selected from the group consisting of hydrogen and C1-10 alkyl. These compounds are useful pharmaceutical agents with improved oral bioavailability.
US7842808 Anti-migraine spirocycles The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
US20080069899 In mixture with drug that prevents Dna reproduction The invention relates to the use of at least one compound of general formula (1) for the production of a medicament for the treatment of cancer.
CA2734588A1 Silver ion delivery platform The present invention pertains to silver ion bearing carriers useful in treating monorrhagia of a mammalian uterus, comprising a physiologically inert, flexible earner, e.g., a coil, bearing a tissue cauterizing amount of a silver ion. Silver ions are delivered to the endometrium and cause necrosis of the endometrial tissue. The silver ions remaining within the uterine cavity can then be neutralized with a sodium chloride solution delivered to the uterus e.g., by catheter, and the carrier recovered from the uterus.
CN102872078A Application of Houttuynoid C in drugs for treating leukemia The invention relates to an application of Houttuynoid C in drugs for treating leukemia, belonging to the field of medicines. The application of Houttuynoid C in drugs for treating leukemia comprises an application of Houttuynoid C in preparing drugs for restraining multiplication of leukemia cells and application of Houttuynoid C in preparing drugs for inducing apoptosis of leukemia cells. Houttuynoid C treats leukemia by restraining the multiplication of leukemia cells and inducing the apoptosis of leukemia cells. The application of Houttuynoid C in drugs for treating leukemia disclosed by the invention is publicized for the first time; and as the skeleton type is brand new, Houttuynoid C has an unexpectedly strong inhibitory activity to leukemia cells.
US20090142292 Method For The Mitigation of Symptoms of Dry Eye A method for the mitigation of symptoms of dry eye is disclosed. The method involves at least (a) incorporating one or more non-functionalized polymers having one or more hydrophilic moieties into an ophthalmic device that is a polymerization product of a comonomer mixture comprising: (i) a major amount of a non-silicone-containing hydrophilic monomer; and (ii) an end terminal functionalized surfactant; and (b) inserting the ophthalmic device in the eye of a patient.
WO2013041696A1 Stimulating and invigorating nasal spray and nasal drop The invention relates to the use of a composition containing at least one ethereal oil and at least one simulating substance for nasal administration. The composition is introduced into the nose, in particular formulated as a nasal spray or nasal drop, but is also suitable for inhalation.
US20090247616 Use of benzo-fused heterocyle sulfamide derivatives for the treatment of anxiety The present invention is a method for the treatment of anxiety and related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined. The present invention is directed to a method for the treatment of anxiety and related disorders, which includes mono-therapy and alternatively, co-therapy with at least one anxiolytic.
EP2091942A1 Substituted pyrazinone derivatives for use as a medicine The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective 2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.
WO2007077929A1 Therapeutic agent for metabolic syndrome and food containing the therapeutic agent Disclosed is a novel therapeutic agent for metabolic syndrome which can ameliorate the accumulation of visceral fat and can prevent/treat metabolic syndrome. The therapeutic agent for metabolic syndrome comprises a dietary fiber aggregate as an active ingredient, wherein the dietary fiber aggregate contains a water-soluble β-glucan in the largest content. A particularly effective example of the water-soluble β-glucan is one having a β-1,3-glycoside bond and a β-1,4-glycoside bond in the molecule.
CN101269036A Doxazosin mesylate sustained-release dropping pill and preparation method thereof The invention discloses a pharmaceutical preparation used for treating essential hypertension and benign prostatic hyperplasia, and particularly relates to a prepared sustained-release oral formulation adopting mesylate doxazosin as the ingredient. The pharmaceutical preparation aims to supplement the deficiency of the prior art and provide a sustained-release mesylate doxazosin dropping pill. The sustained-release mesylate doxazosin dropping pill overcomes the defects in the prior art effectively, guarantees no occurrence of an obvious quality change for the drug during the effective storage period and has the advantages of controllable release time, full release and high bioavailability simultaneously.
US20060233724 Medicinal composition for peridontal pocket administration containing bisphosphonic acid derivative or its salt as the active ingredient A pharmaceutical composition for being administered to periodontal pockets, comprising as an effective ingredient a bisphosphonic acid derivative, which has an excellent sustained-release property when locally administered, is disclosed. The pharmaceutical composition for being administered to periodontal pockets according to the present invention comprises a bisphosphonic acid derivative or a salt thereof, and a base which undergoes liquid-gel phase transition upon contacting with physiological body fluid in the periodontal pocket.
CN101601651A Methylprednisolone aceponate lipidosome cream The invention relates to a lipidosome medical composition which uses methylprednisolone aceponate as an active component, and a cyst diameter of lipidosome is smaller than 800 nm. The composition comprises 0.025 percent to 0.2 percent of methylprednisolone aceponate as the active component, 0.5 percent to 6 percent of phospholipid, 0 percent to 1 percent of lipophilic additive, 0.01 percent to 1 percent of antioxidant which is used for preserving the medical composition, a pH buffering agent which is used for retaining the pH value from 5 to 7.5, 3 percent to 15 percent of humectant, 20 percent to 30 percent of oil phrase component, 0.01 percent to 0.1 percent of antimicrobial preservative and the balanced of water. The methylprednisolone aceponate lipidosome cream is used for treating skin diseases of human beings or animals.
CN101544681A New anti-tumor compound holothuria nobilis selenka saponin octyl of holothuria nobilis selenka The invention relates to an anticancer compound holothuria nobilis selenka saponin octyl separated from holothuria nobilis selenka, belonging to the technical filed of medicines. A molecular formula of the anticancer compound holothuria nobilis selenka saponin octyl is C54H86O24, and a spatial configuration of the chemical construction of the anticancer compound holothuria nobilis selenka saponin octyl is determined by a plurality of modern spectral analysis methods and especially determined by the comprehensive analysis of advanced two-dimensional NMR spectra and high resolution mass spectrography. An in-vitro anti-tumor test shows that the anticancer compound holothuria nobilis selenka saponin octyl has obvious inhibitory action on two tumour cell strains, i.e. an A-549 lung cancer and an IA-9 ovarian cancer. The invention can provide lead compounds for developing a new anti-tumor medicine, thereby having the magnificent meaning for developing and utilizing Chinese ocean medical living resources.
CN102114025A Pharmaceutical composition for treating osteoporosis The invention belongs to the technical field of medicine, and discloses a pharmaceutical composition for treating osteoporosis. The pharmaceutical composition for treating osteoporosis comprises minodronate as raw material and adjuvants, wherein minodronate is micronized minodronate. On the basis of deep study on the physical and chemical properties of minodronate, the scientific personnel of our company found by accident that the minodronate preparations prepared by the steps of micronizing minodronate to obtain minodronate of a certain particle size and making into preparations have the advantages of uniform quality and good dissolution.
US7173040 4-phenyl-6-alpha-(imidazolyl-, 1,2,4-triazolyl- or pyridyl)-benzyl substituted This invention comprises the compounds of formula (I): wherein r, s, t, Y1–Y2, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
US20120258948 N-Linked Hydroxamic Acid Derivatives Useful As Antibacterial Agents The present invention is directed to a new class of hydroxamic acid derivatives of formula I, wherein the variables G, T, D, L, R1, R2, R3 are as described herein, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections in a patient in need thereof.
US7994346 such as methyl 2-({(4S,5R)-5-[(1E,3E,7E)-(S)-10-(4-fluorophenoxy)-9-hydroxydeca-1,3,7-trien-5-yn-1-yl]-2,2-dimethyl-1,3-dioxolan-4-yl}methoxy)acetate, useful in treating inflammatory and autoimmune disorders in humans This invention is directed to compounds useful as intermediates in the synthesis of lipoxin A4 analogs of the following formulas (I) and (II): wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.
WO2007124668A1 Pharmaceutical composition comprising high concentrate of polydatin A pharmaceutical composition comprising high concentrate of polydatin. The composition contains polydatin, meglumine and/or cyclodextrin. The said composition is in the form of aqueous solution or lyophilized product which is to be prepared before using.
US20060205722 Such as N-{1-[2-(1,3-dioxan-2-yl)ethyl]piperidin-4-yl}-N-(4-fluorobenzyl)-2-[4-(2-hydroxy-2-methylpropoxy)phenyl]acetamide; selective inverse agonists of 5-HT2A receptor with minimal monamine receptors subtype activity; antipsychotics with reduced side effects Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.
US20120289597 Nitric oxide amino acid esters for the treatment of chronic pain There is provided a topical composition and a method for treating or alleviating pain in a patient in need thereof. The topical composition contain amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof and a topical analgesic compound.
WO2013002485A3 Pharmaceutical composition for preventing and treating kidney disorders, containing inhibitor for phosphorylation of taz tyrosine as active ingredient for activation of nfat5/tonebp The present invention relates to a pharmaceutical composition for preventing and treating kidney disorders caused by osmotic stress, containing an inhibitor for the phosphorylation of TAZ tyrosine as an active ingredient. More specifically, it has been ascertained that TAZ inhibits the activity of NFAT5/TonEBP, the activity of c-Abl is required for the interaction between TAZ and NFAT5/TonEBP, phosphorylated TAZ inhibits the binding activity of NFAT5/TonEBP, and the inhibition of TAZ maximizes the expression of a target gene and the activity of NFAT5/TonEBP for relieving the influence of a hypertonic stimulus under in vivo hypertonic conditions caused by dehydration, and thus the inhibitor for phosphorylation of TAZ tyrosine can be useful for preventing or treating kidney disorders caused by osmotic stress.
CN102250204A RGD sequence peptidyl methyl curcumin compounds, preparation method thereof, and application thereof The invention provides a type of RGD sequence peptidyl methyl curcumin compounds, which are 1-(3,4-dimethoxyphenyl)-7-(4-acetoxide RGD sequence peptidyl-3-methoxyphenyl)-1,6- heptadiene-3,5-diketone compounds (RGD=Arg-Gly-Asp). The invention also provides a preparation method of the compounds. Through experiments, platelet aggregation resisting effects of the compounds in platelet aggregation in vitro models and antithrombosis resisting effects of the compounds in rat carotid artery and jugular vein bypass intubation thread method models are verified. Therefore, 1-(3,4-dimethoxyphenyl)-7-(4-acetoxide RGD sequence peptidyl-3-methoxyphenyl)-1,6-heptadiene-3,5-diketone provided by the invention has clinic application prospects to be applied as antithrombotic agents.
US20110065662 Compounds, Compositions, and Methods for Protecting Brain Health in Neurodegenerative Disorders Aspects of the invention relate to compounds, extracts and compositions thereof, and methods of using of the same, to treat neurodegenerative disorders and/or improve brain health. In certain embodiments, said compounds are pomegranate flavonoids.
CN103126800A Zinc-citric acid heating system in medicinal compressing patch The invention discloses a zinc-citric acid heating system in a medicinal compressing patch and belongs to the technical field of medicinal compressing patches. The zinc-citric acid heating system is prepared by following ingredients: zinc powder, citric acid, rheumatism removing solution, rheumatism removing powder and activated carbon. The zinc-citric acid heating system in the medicinal compressing patch has the advantages of large medicine-carrying amount, stable nature in oxidation products, freeness of interaction with other medicine and freeness of generation of undesirable odors.
WO2012165854A9 Long interfering dsrna simultaneously inducing an immune reaction and the inhibition of the expression of target genes The present invention relates to a long interfering dsRNA (liRNA) capable of promoting an immune reaction as well as inhibiting the expression of specific RNAi-mediated target genes, and to uses thereof. More particularly, the present invention relates to a long interfering dsRNA capable of inducing the expression of interferon-β by stimulating, depending on a structure, a protein kinase R (PKR) path as well as inhibiting the expression of specific target genes through an RNA-interfering reaction through a specific sequence.
CN101486643B Trans naproxen ester, optical isomer thereof, as well as preparation and use thereof The invention discloses a naproxen isopropyl ester (I) or an optical isomer (II) thereof that has the chemical formula showed as follow. The preparation method of the naproxen isopropyl ester is as follows: 6-methoxyl-2-naphthyl ethanone and onium salt inside sulfonium generate 2-(6-methoxyl-2-naphthyl) propylene epoxide through epoxidation and esterification is conducted to 2-(6-methoxyl-2-naphthyl) propanol obtained through palladium-carbon catalytic hydrogenolysis and carboxylic acid or acyl chloride to produce naproxen isopropyl ester. The preparation method of the optical isomer (S)-naproxen isopropyl ester is as follows: (S)-2-(6-methoxyl-2-naphthyl) propanol is obtained through the esterification of (S)-naproxen and lithium borohydride reduction; or lithium aluminium hydride is adopted to reduce naproxen to get (S)-2-(6-methoxyl-2-naphthyl) propanol; and esterification between (S)-2-(6-methoxyl-2-naphthyl) propanol and carboxylic acid or acyl chloride is carried out to obtain (S)-naproxen isopropyl ester. The naproxen isopropyl ester or the optical isomer thereof can be applied to preparing anti-inflammatory analgesics.
US20080194517 Equine or canine immunomodulating composition and treatment method An equine or canine immunomodulating composition comprises a pre-packaged, feed supplement comprising effective amounts of a beta-glucan mixture which is at least 60 percent purified. The feed supplement may be a dry feed supplement further including (b) an effective amount of at least one flavoring, and (c) an effective amount of a sweetener. The feed supplement may include an effective amount of an antioxidant; and an effective amount of an emulsifier. An alternative composition further comprises an appetite stimulant. A method of treating equine or canine microbial infections following the diagnosis of a microbial infection comprises the step of treating the equine or canine for a period at least long enough to prevent immediate recurrence of the microbial infection with effective amounts of the immunomodulating composition described above. The immunomodulating composition may alternatively be used in combination with an effective amount of an antibiotic.
CA2556801A1 Methods and agents for inhibiting dynamin-dependent endocytosis There are disclosed methods for inhibiting dynamin-dependent endocytosis in cells comprising treating the cells with an effective amount of a compound of formula (I), or a dimeric tyrphostin, physiologically acceptable salt, or prodrug thereof. Compounds useful in the methods described are also provided. The inhibition of dynamin-dependent endocytosis of cells is applicable to the treatment of epilepsy and neurological disorders and conditions.
US20120276198 Pharmaceutical composition for treating parkinson's disease and preparation method thereof A pharmaceutical composition used to treat Parkinson's disease contains levodopa, carbidopa and entacapone or pharmaceutically acceptable salt thereof, and at least one kind of pharmaceutically acceptable excipients. Entacapone is not mixed with levodopa or carbidopa in the pharmaceutical composition. The preparation method of the pharmaceutical composition includes making the first particles with levodopa and carbidopa, making the second particles with entacapone, and then pressing the two kinds of particles into tablets.
WO2006008316A2 Selective inhibitors of human corticosteroid syntheses The invention relates to compounds for selectively inhibiting human corticosteroid syntheses CYP11B1 and CYP11B2, to the production thereof and to their use for treating hypercortisolism and diabetes mellitus or insufficiency of the heart and myocardial fibrosis.
US20080279846 lipoprotein-associated phospholipase A2 (Lp-PLA2) The present invention provides compostions and methods useful for treating and preventing neurodegenerative disease and neurologically related disorders by inhibition of Lp-PLA2. The compositions and methods are useful for treating and preventing diseases and disorders with abnormal blood brain barrier (BBB) function, for example neurodegenerative diseases with a permeable BBB, such as but not limited to, Alzheimer's Disease, Huntington's Disease, Parkinson's Disease and Vascular Dementia.
CN103393699A Application of Chukrasone A in preparing medicines for treating rhinitis The invention relates to Chukrasone A for treating immune-inflammation, which is used for preparing medicines for treating immune-inflammation, and particularly used for preparing medicines for treating rhinitis. By using terfenadine and diclofenac sodium as control, Chukrasone A is exact in curative effect. The use of Chukrasone A in preparing medicines for treating rhinitis provided by the invention is disclosed for the first time. As the framework type is a brand-new framework type, the activity of treating rhinitis is unexpectedly strong, and the probability of giving any enlightenment by other compounds does not exist, so that Chukrasone A has remarkable substantive characteristics, and meanwhile has a remarkable progress for preventing and treating rhinitis.
US20110118199 Use of cns penetrating anticancer compounds for the treatment of protozoal diseases The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.
CN103463581A Preparation method and application of cholagogic and lithagogue tablet The invention provides a preparation method of a cholagogic and lithagogue tablet. The raw materials include 250g of desmodium, 250g of oriental wormwood, 75g of scutellaria baicalensis, 75g of elecampane, 75g of curcuma aromatica, 125g of rheum officinale, 125g of betel nuts, 50g of immature bitter oranges, 25g of mirabilite and 50g of cortex magnoliae officinalis made of ginger. The tablet is prepared through supercritical extraction, therefore, the content of the effective constituents is greatly improved, and the dose is reduced. The invention further provides application of the cholagogic and lithagogue tablet in preparation of medicine for suppressing human lung adenocarcinoma GLC-82 cell proliferation.
WO2006040281A1 Thiazolyl-dihydro indazoles The invention relates to the compounds of general formula (1), wherein R1 to R3 are defined as in claim 1, which are suitable for use in the treatment of diseases that are characterized by excessive or abnormal cell proliferation. The invention also relates to the use of said compounds for producing a drug having the aforementioned properties.
CA2358436C Polyunsaturated fatty acid derivatives and their use Novel amides are disclosed, in particular amides of the all-trans-retinoic acid or 13-cis-retinoic acid and arachidonic acid and docosahexaenoic acid and eicosapentaenoic acid or linoleic acid with 2-aminoethanol, alpha-L-serine, alpha-L-threonine, alpha-L-tyrosine containing phosphate groups. Further, the present invention discloses the synthesis and use of these compounds, in particular their pharmaceutical application.
CN101239901A Method for preparing ibuprofen arginine salt The invention discloses a method for preparing ibuprofen arginine salts. In the invention, arginine is added in ibuprofen ethanol sollution under the ambient temperature and agitation, salt precipitation and crystallization are performed in a container in order. The preparing process is simple, convenient, high in yield, good in reproduction. The ibuprofen arginine salts can be used in preparing oral preparations and injections, is good for quickening adsorption speed, increasing bioavailability and enlarging application range.
US20100303908 Pharmaceutical composition comprising desloratadine The present application relates to pharmaceutical compositions comprising desloratadine and a pharmaceutically acceptable polymer.
WO2011026912A3 Retinoic acid receptor antagonists, mir-10a inhibitors and inhibitors of hoxb1 or hoxb3 repressors for treating pancreatic cancer The present invention relates to miR-10a inhibitors or inhibitors of HOXB1 and/or HOXB3 repressors for the treatment of pancreatic cancer.
WO2012142476A2 Methods and compositions for the treatment of marfan syndrome and associated disorders The instant invention provides methods and compositions for the treatment and prevention of Marfan syndrome and related diseases, disorders and conditions. The invention further provides pharmaceutical compositions and kits for the treatment and prevention of Marfan syndrome and related diseases, disorders and conditions.
WO2008092861A1 Bicyclic derivatives as ep4 agonists The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein ring E represents a partiallysaturated or aromatic 5-membered heterocycle wherein the dotted lines represent an optional double bond and wherein B, C and D each independently represents CH 2, CH, N, NH, S or O and F represents N or C, provided that the 5-membered ring contains 1, 2 or 3 heteroatoms; X represents a direct bond or C 1-4alkanediyl; Y represents N or CH; R1 represents hydrogen or fluoro; R2 represents hydrogen, halo, cyano, C 1-6alkyl, C 1-6alkyloxy, C 1-6alkylcarbonyl or C 1-6alkylcarbonylamino; R3 represents hydrogen, halo, C 1-6alkyl, C 1-6alkyloxy, cyano, nitro, amino or mono-or di(C 1-6alkyl)amino; R4 represents halo; hydroxyl; carboxyl; optionallysubstituted C 1-6alkyl; polyhaloC 1-6alkyl; C 1-6alkyloxycarbonyl; polyhaloC 1-6alkyloxy; optionallysubstituted C 2-6alkenyl; cyano; nitro; NR10 R11; C 1-6alkylthio; optionally substituted C 1-6alkyloxy; or two adjacent R4 substituents may be taken together; n represents an integer of value 1, 2 or 3; m represents aninteger of value 1, 2 or 3; provided that R3 may onlybe other than hydrogen if at least one of R1 or R2 is other than hydrogen; and provided that2,6- bis(1,1-dimethylethyl)-4-[6-(2-phenylethoxy)-1H-purin-2-yl]-phenol is not included; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a disease by activating the EP4 receptor.
WO2013043580A3 Modified creatine compounds The invention discloses creatine derivatives that are represented by Formula (I), Formula (II), and Formula (III); wherein Z is a functional group; Y is a mitochondrial targeting agent, a cationic ammonium group, or a polypeptide containing at least one positively charged amino acid residue; each R1 is independently hydrogen, alkyl, or a phosphate group; R2 a linker; R3 is a spacer group; R4 is hydrogen, alkyl, aryl, or heterocyclic; or R4 and R1, or R4 and R3, together with the nitrogen atoms to which they are attached form a heterocyclic ring, and W is hydrogen or alkyl.
US7074808 4-(Phenyl-piperidin-4-ylidene-methyl)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestional disorders Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, pyrroloyl, thienyl, furanyl, imidazolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6 alkyl, NO2, CF3, C1–C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.
US20120316185 Cyclohexyl Amide Derivatives as CRF Receptor Antagonists There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).
WO2013052465A1 [1,3]dioxolo[4,5-g]quinoline-6(5h)thione and [1,3]dioxolo[4,5-g][1,2,4]triazolo[1,5-a]quinoline derivatives as inhibitors of the late sv40 factor (lsf) for use in treating cancer The present invention relates generally to [l,3]dioxolo[4,5-g]quinoline-6(5H)thione and [1,3]dioxolo[4,5-g][1,2,4]triazolo[1,5-a]quinoline derivatives and/or compositions for use in inhibiting, preventing and/or treating cancer, e.g. hepatocellular carcionoma (HCC). In some embodiments, the invention relates to the use of small-molecule compounds to inhibit, prevent and/or treat expression of the transcription factor Late SV40 Factor (LSF) for treatment of HCC or other cancer types.
CN103108631A Pharmaceutical combination for the treatment of pain The present invention relates to a combination comprising as components (a) at least one 3-(3-Dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and (b) at least one NMDA-antagonist, a pharmaceutical formulation and a dosage form comprising said combination as well as a method of treating pain, e.g. inflammatory pain or neuropathic pain, wherein components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.
WO2013106238A1 Leukotriene b4 antagonist compound The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also, the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The present invention further provides methods for treating abdominal aortic aneurysm or atherosclerosis comprising administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of Formula (I) or pharmaceutically acceptable salt thereof.
EP1509207A1 Pharmaceutical composition containing oxcarbazepine and having a controlled active substance release The invention relates to pharmaceutical compositions, particularly oral compositions, containing an effective content of oxcarbazepine and having a delayed active substance release. The compounds have a characteristic in-vitro release profile.
CN102600066A Temperature sensitive gel sustained-release oral agent with paracetamol The invention discloses a temperature sensitive gel sustained-release oral agent with a paracetamol, and relates to the technical field of pharmaceutic preparation. A carrier in the oral agent provided by the invention convenient for feeding includes paracetamol serving as an active ingredient and xyloglucan or a mixture of xyloglucan and another polysaccharide, wherein another polysaccharide is pectin, chitosan, algal polysaccharides or gellan gum. According to the invention, a polymer three-dimensional gel net structure formed by the polysaccharide is used for establishing a sustained-release system combined with clinical pathology so as to obtain the temperature sensitive gel sustained-release oral agent with the paracetamol; the temperature range for sol-gel change is 35-37 DEG C which is close to body temperature, so the oral agent is particularly suitable for old people, infants and people who have difficulty in swallowing, and has obvious efficacy. The temperature sensitive gel sustained-release oral agent disclosed by the invention has obvious analgesic and antipyretic effects, is convenient for administration and free of toxic and side effects, and the drug action can last for a long time.
CN103655571A Lopinavir and ritonavir compound high-uniformity nano co-dispersion body and preparation method thereof The invention provides a lopinavir and ritonavir compound high-uniformity nano co-dispersion body. The lopinavir and ritonavir compound high-uniformity nano co-dispersion body consists of lopinavir and ritonavir which are taken as active ingredients, a dispersing aid, an anti-agglormeration material, a dispersing stabilizer, a dispersion supporter and a lubricant. The lopinavir and ritonavir which are taken as active ingredients account for 25%-60%. The lopinavir and ritonavir compound high-uniformity nano co-dispersion body prepared by the preparation method disclosed by the invention can be prepared into a single-dose preparation according to a normal method. According to a dissolution rate experiment, the preparation disclosed by the invention has release amount of 40%-80% within 30 minutes. The preparation prepared by the dispersion body disclosed by the invention is high in dissolution rate, and can be used for improving the bioavailability. The lopinavir and ritonavir compound high-uniformity nano co-dispersion body prepared by the preparation method disclosed by the invention satisfies and is superior to mixing uniformity standards. The preparation method disclosed by the invention is simple and easy to implement, can be used for popularizing application of a nano mechanical grinding technology on the pharmaceutical industry and promoting the development of the technology, and is suitable for industrial production and greater in application value.
US7319109 4-(Substituted phenoxy or anilino)-3-phenyl- or phenylalkylisoxazoles: 3-{[(4-{[3-(2,6-Dichlorophenyl)-5-isopropylisoxazol-4-yl]methoxy}-2-methylphenyl)-(methyl)amino]methyl}benzoic acid; cardiovascular disease, cholestatic liver disease, organ fibrosis, triglycerides, increasing high density lipoprotein The invention relates to a compound of formula (I): wherein all variables are as defined herein and to pharmaceutical compositions, methods of using, and processes for preparing the same.
US20080161346 Pyridines or pyrimidines having 4-(hydrogenated 1-pyridyl- or hydrogenated 1-isoquinolyl rings, e.g., N-(4-chlorophenyl)-2-(pyridin-4-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide; kinase inhibitors; inflammation, angiogenesis and cancer Selected compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
US20120076847 Medical instrument and method of manufacturing the same A medical instrument and a manufacturing method thereof are provided. The medical instrument includes a biomedical metal layer and a polymer film. The polymer film is a biodegradable polymer material. The manufacturing method includes the following steps: providing the biomedical metal layer, immersing the biomedical metal layer in a polymer solution, performing a baking process on the biomedical metal layer coated with a polymer film, forming the biomedical metal layer coated with the polymer film, taking out the biomedical metal layer coated with the polymer film to fabricate the medical instrument. The biodegradable polymer film and the biomedical metal layer are combined into the medical instrument, so that a physician performs a surgery more easily. In addition, decomposition time of the polymer film can be preset, so as to achieve efficacy of blocking soft tissue cells having a higher growth rate.
US20070287715 e.g.5-(4-tert-Butylphenyl-1-(4-(2-carboxypropan-2-yloxy)phenyl)indole-2-carboxylic acid ; inhibition of the activity of microsomal prostaglandin E synthase-1, 5-lipoxygenase-activating protein (FLAP); respiratory system disorders There is provided a compound of formula: (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.
US20090298805 Topical pyrithione compositions and methods for treatment of nail fungus Disclosed is a formulation and method for the treatment of fungal infections of the nail (onychomycosis) utilizing a topical composition comprising zinc pyrithione, a solubilizer for the zinc pyrithione, a film former, and a volatile solvent. The formulation is preferably in the form of a lacquer. The composition containing the metal pyrithione complex is topically applied to the infected nail preferably as a nail polish or lacquer which may be applied with a dropper, swab or the like to the afflicted nail surface. The treatment can be done at least two times a day, with a course of treatment lasting from several weeks to several months or until a cure is effected or a significant reduction of the infection is achieved.
EP1711494B1 Aryl substituted heterocycles, method for production and use thereof as medicaments The invention relates to substituted, aryl-substituted heterocycles, the physiologically-acceptable salts and physiologically-functional derivatives thereof, methods for production and use thereof as medicaments. Compounds of formula (I), where the groups have the given meanings, the N-oxides and physiologically-acceptable salts thereof and methods for production thereof are disclosed. The compounds exhibit, for example a weight-reducing effect in mammals and are thus suitable for use in, for example, prevention and treatment of obesity and diabetes. Said compounds are MCH receptor antagonists.
US20120108509 Artificial scab for use in an airway Body tissue and structures in an airway may be treated with an artificial scab comprising an inhomogeneous, uncohesive, solid sheet-like body comprising a granular mixture of chitosan and polysaccharide particles. The artificial scab breaks apart into smaller pieces if peeled away from the surgical site or wound, thus reducing the risk of airway occlusion.
US20070298999 Method for treating pain with a calmodulin inhibitor The present invention relates to the use of Ca2+/CaM-dependent protein kinase II (CaMKII) inhibitors alone and in combination with opiate analgesics for treating pain, in particular chronic pain. Methods for reducing or reversing tolerance and dependence on opiate analgesics are also provides.
WO2014095489A1 Topical oral composition for alleviating dry mouth symptoms and for treating mouth ulcers The invention concerns a topical oral composition comprising taurine, propanediol and xylitol and its use for alleviating or eliminating symptoms of dry mouth and/or preventing or treating mouth ulcers.
WO2007026533A1 Soluble tablet containing nanosilicon particles and process for production thereof Disclosed is a tablet comprising a sodium chloride powder and an abundance of nanosilicon particles having a particle size in the range of 1.5 to 2.0 nm, 2.0 to 2.5 nm or 2.5 to 3.5 nm blended into the powder, which can emit a fluorescent light with blue, green or red color in the blood upon being irradiated with ultraviolet ray or visible light. The tablet can be produced by immersing nanosilicon particles in a mixed solution containing a therapeutic agent and a polymeric compound such as a polysaccharide or protein, subjecting the resulting mixture to a thermal treatment and then mixing the resulting product with a sodium chloride powder.
CN103356553A Application of Sarcaboside A in preparation of drug for treating breast cancer The invention discloses application of Sarcaboside A in preparation of a drug for treating breast cancer, which belongs to the technical field of new applications of drug. According to the invention, the in-vitro MTT (Methyl Thiazolyl Tetrazolium) antitumor activity evaluation discovers that Sarcaboside A also has an obvious inhibiting effect on the growth of human breast cancer cell strains 4T1, MCF-7, MDA-MB-231 and MCF-7B. Thus, Sarcaboside A can be used for preparing an anti-breast cancer drug and has good development and application prospects. The application of Sarcaboside A in preparation of the drug for treating breast cancer is disclosed by the invention for the first time. The skeleton type is brand new and Sarcaboside A has unexpectedly strong inhibitory activity to the human breast cancer cell.
US20110034412 Visually observable material for medical treatment A visually observable material for medical treatment, which is preferable as an adhesion preventive material and a hemostatic material for biological organisms includes a crosslinking composition comprising at least two components of a crosslinking polysaccharide derivative with an active ester group reactive with active hydrogen in the co-presence of an alkali, where the active ester group is preliminarily introduced in a side chain of a polysaccharide and the crosslinking polysaccharide derivative is not yet crosslinked, and a carbonate including at least one type of carbonate generating divalent carbonate ion in an amount at a mass ratio of 0.03 or more to the polysaccharide derivative.
CN1781527A Xingnaoling magic plaster The present invention discloses a kind of externally applied medicine with the functions of clearing away heat, diminishing inflammation, relieving pain and refreshing. The magic Xingnaoling plaster is one kind of transdermal absorbed preparation with scientific Chinese and Western combined recipe. The present invention has the advantages of simple preparation process, low cost, convenient use, fast acting, etc.
CN103371994A Medicine for treating melanoma and application thereof The invention discloses a medicine for treating melanoma. The medicine comprises a compound shown in a chemical formula I or a pharmaceutically acceptable salt of the compound, wherein the chemical formula I is shown in the specification; in the formula I, R1 is F, Cl, Br or I, R2 is H or alkyl of C1-C3, and R3 is H or alkyl of C1-C3. The experiment data of the specific embodiments show that the medicine for treating melanoma has strong specificity but low toxicity.
WO2009025792A2 Crystalline forms cinacalcet fumarate and cinacalcet succinate and processes for preparation thereof The present invention provides crystalline forms of Cinacalcet Fumarate and Cinacalcet Succinate, pharmaceutical compositions comprising the crystalline form of Cinacalcet Fumarate and/or the crystalline form of Cinacalcet Succinate, and processes for preparing the crystalline forms of Cinacalcet Fumarate and Cinacalcet Succinate and pharmaceutical compositions comprising the crystalline forms.
CN101422448A Miconazole nitrate film and preparation method and pharmacy use thereof The invention discloses a new preparation formulation-a film agent of miconazole nitrate, which is made by miconazole nitrate, film-forming material, a plasticizer, a film material lytic agent and an antiseptic according to certain weight ratio; a preparation method thereof comprises the following four steps: step I. proper amount of the film material lytic agent is added into the film-forming material, fully mixed and then rested for being fully expanded; step II. the film material lytic agent is added into the miconazole nitrate to lead the miconazole nitrate to be dissolved, then the plasticizer is added to lead the miconazole nitrate to be clarified; step III. the film-forming material in step I is arranged in water bath and heated; proper amount of plasticizer is added and evenly mixed with the antiseptic; the main medicament dissolved in step II is added and arranged on the water bath, heated and evenly stirred; and step IV. the medicine slurry is evenly paved on a glass board by a board scraping method, blown and dried for 5 to 10min, thus instantly forming the film. The film agent of miconazole nitrate prepared by the invention is characterized by small size, light weight, convenient use, high safety and good stability, as well as long residual action and quick effect; moreover, the preparation technique is simple and the maneuverability is high.
WO2009084743A1 External preparation for preventive or therapeutic use An external preparation containing an active hydrogen-generating agent which generates active hydrogen in the case of bringing a plural number of agents into contact with each other and/or an active hydrogen-generating agent which activates hydrogen molecules thus generated.
WO2009055859A1 Transdermal delivery system for hormones and steroids A transdermal delivery system comprising a composition comprising a pharmacological agent and a penetration enhancer wherein the penetration enhancer comprises polyethylene glycol (PEG) of average molecular weight no more than 300.
CN1879703A An externally applied medicine for treating hicismus Disclosed is an externally applied medicine for treating tragomaschalia, which is prepared from the following raw materials: lead monoxide, Radix Cinnamomi Camphorae, clove, boneol and 75% ethanol.
US20050004167 Such as dibenzofuran-2-carboxylic acid 2-(phenylsulfonyl)hydrazide The invention relates to BCAT inhibitor compounds of formula (I) and use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
WO2011159857A1 Carboline carboxamide compounds useful as kinase inhibitors Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.
US20120059052 Prenylflavonoid formulations Methods and formulations for increasing the water solubility and/or bioavailability of prenylfiavonoids are disclosed. The formulations may be employed to treat a disease states, including cancer.
CN103145571A Crystal form of derivative of aminomethyl caproic acid The invention discloses a crystal form of a derivative of aminomethyl caproic acid, and in particular discloses a compound with the following structural formula. The compound determined by an X-ray diffractometer in a diffraction pattern has diffraction peaks at about 9.05 degrees and the like. The compound provided by the invention can be used for auxiliary treatment of generalized anxiety disorder, diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia syndrome and epilepsia.
US20080090848 Substituted Purinyl Derivatives With Immunomodulator And Chemoprotective Activity And Use Alone Or With Medium-Chain Length Fatty Acids Or Glycerides The present invention describes new biological activities of immunomodulating 6-substituted purinyl compounds which make them particularly useful during the treatment of cancer. Collectively, these new biological activities make these purinyl compounds useful chemoprotective agents for the treatment of myelosuppression which is associated with cancer chemotherapy and/or radiotherapy. This chemoprotective activity is in addition to the immunomodulating and subsequent anticancer activity displayed by these compounds. The chemoprotective usefulness of these compounds is further enhanced by the use of medium-chain fatty acids or salts or triglycerides or mono- or diglycerides in combination with the 6-substituted purinyl compounds of this invention.
CN102898417A Benzo-hexahydric nitrogenous heterocycle derivative The invention belongs to the medicine technical field, more specifically relates to a cyclic compound, its pharmaceutically acceptable salt, its stereisomer or its solvent compound shown in a general formula (I), wherein R<1>, R<2>, R<3>, X, Y and Ar are defined as an instruction. The invention also relates to a preparation method of the compounds, a pharmaceutical composition containing the compound, and an application of the compound and the pharmaceutical composition in the preparation treatment and/or prevention of the inflammation diseases such as the inflammation diseases which take the undesirable inflammation-immune response as a characteristic or are related with the undesirable inflammation-immune response, and the diseases which are related with the symptoms and states of an illness due to hypersecretion of THF-alpha and PDE-4 or related with hypersecretion of THF-alpha and PDE-4.
CN1939263A Oral preparation containing cefaclor and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains cefaclor. Its preparing process is also disclosed.
WO2012105219A1 Antibody therapy effect-enhancing drug In recent years, antibody drugs have garnered interest as a cancer treatment, but while in some cases the activity of the antibodies was too weak to achieve sufficient treatment results, in other cases, high dosage amounts led to too high a cost burden on patients. For that reason, increasing immune activity has become an important issue for antibody therapy drugs, and there is need for an antibody treatment adjuvant capable of enhancing the effect of antibody drugs and thereby suppressing the amount thereof used. If lymphocytes can be made to migrate and collect in and around a tumor, the effectiveness of an antibody drug may be further improved. The purpose of the present invention is to provide a safe and low-cost antibody treatment adjuvant therapy drug capable of enhancing the effect of antibody drugs. Implantation of a dense body of β-tricalcium phosphate (TCP) into the body functions to allow activity, migration and accumulation of immune cells. The inventors discovered that the therapeutic effect of antibody drugs can be enhanced by utilizing this function, which led to the perfection of the present invention.
EP1289923B1 Epithelial cell cancer drug A method of treating epithelial cell cancer comprising administering to a mammalian patient diagnosed as having an epithelial cell cancer a therapeutically effective amount of 4,5 di-cyclo, disilico, dimagnesium, dialumino, oxyo, trihydrate, or its acetate, sulfate, hydrochlorate, or brominate salts. The composition is synthesized from a naturally occurring non-toxic zeolites, and has a 100% kill rate within 72 hours against buccal mucosa and ling squamous epithelial cell cancers. It is not cytoxic to healthy human cells.
US7618979 Prostaglandin receptor antagonists; allergic rhinitis, nasal congestion and asthma; [5-[(4-chlorophenyl)thio]-4-(methylsulfonyl)-6,7,8,9-tetrahydropyrido[3,2-b]indolizin-6-yl]acetic acid Pyridopyrrolizine and pyridoindolizine derivatives are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
EP2133335A1 Sphingosine compound, method for producing the same, and sphingomyelinase inhibitor An object of the invention is to provide a novel sphingosine compound with an inhibitory activity against sphingomyelinase, and a method for producing the sphingosine compound. The novel sphingosine compound or a salt thereof according to the invention is represented by Formula (1): wherein one of R1 and R2 is hydrogen, and the other is a group represented by Formula (G): wherein n is 0 or 1; and R3 is hydrogen, C1-23 alkyl, C3-8 cycloalkyl, C2-6 alkenyl, C1-6 alkoxy, C3-8 cycloalkyloxy, phenyl, or furil.
US20060257392 Remedy or preventive for low turnover bone diseases An agent for treating or preventing low-turnover bone diseases, comprising as an active ingredient a spherical activated carbon, is disclosed. The low-turnover bone diseases include renal osteodystrophy and adynamic bone disease, caused by a low-turnover bone. The adynamic bone disease includes adynamic bone disease in conservative chronic kidney disease, and renal osteodystrophy in a patient under treatment with dialysis.
US8580802 Pyrrolo[2,3-D]pyrimidines as inhibitors of Janus kinases The present invention relates to compounds of the following structural formula: which are useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
CN102755304A Preparation method of guaifenesin and dextromethorphan hydrobromide capsules The invention discloses a preparation method of guaifenesin and dextromethorphan hydrobromide capsules. The method includes the following steps: A, respectively sieving guaiacol glycerin ether, dextromethorphan hydrobromide and dextrin with the amount according to the prescription through a 100-mesh sieve, and evenly mixing the guaiacol glycerin ether, the dextromethorphan hydrobromide and the dextrin; B, performing dry granulating on the mixture obtained through the step A; C, sieving particles with meshes of 16-60 in the step B, adding magnesium stearate with the amount according to the prescription, evenly mixing, filling, polishing and performing bubble capping to obtain the guaifenesin and dextromethorphan hydrobromide capsules. The preparation method is ingenious in design, simple in process, small in raw material consumption and high in product yield and effectively reduces production cost.
CN101815724A aprotinin-like polypeptides for delivering agents conjugated thereto to tissues Based on our identification of a polypeptide (Angiopep-7) that is efficiently transported to cells such as liver, lung, kidney, spleen, and muscle, the invention provides polypeptides, conjugates including the polypeptides, and methods for treating diseases associated with these cell types. Unlike other aprotinin related polypeptides identified herein (including Angiopep-3, Angiopep-4a Angiopep-4b Angiopep-5, and Angiopep-6) which efficiently cross the blood-brain barrier (BBB), Angiopep-7 is not efficiently transported across the BBB.
CN103319468A Substituted spirobicyclic compounds, and application method and applications thereof The invention provides spirobicyclic compounds possessing the structure of formula (I), pharmaceutically acceptable salts, and medicinal preparations of the compounds, which are used to adjust protein kinase activity and signal response between or in cells. The invention also relates to pharmaceutical compositions containing the compounds, and a method for treating hyperproliferative diseases of mammals especially mankind by using the pharmaceutical compositions.
US20070255061 5-Fluoro-, Chloro-and Cyano-Pyridin-2-Yl-Tetrazoles as Ligands of the Metabotropic Glutamate Receptor-5 The present invention relates to new compounds of formula I, wherein Z, Q, X1, X2, R1 and R2, are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
WO2013113860A1 Fused pyrroledicarboxamides and their use as pharmaceuticals The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.
CN1876641A Method for purifying salvianolic acid B The invention relates the method of extracting purification pellet phenolic acid B from Sage plant, especially extracting purification pellet phenolic acid B from salvia miltiorrhizae. The method comprises the following steps: treating the salvia miltiorrhizae in microwave field for 1-10 minutes, adding water, or disintegrating salvia miltiorrhizae to 10-60 mesh, and adding water, treating it in microwave field for 1- 20 minutes, centrifuging, removing deposition, then carrying out chromatography with polyamide, removing impurity with water and 20-50% alcohol, washing pellet phenolic acid B with 60-80% alcohol, decompressing, thickening, freezing, drying and getting pellet phenolic acid B whose purify is above 95%. The invention has the advantages of simple technology, low cost, high purify and stable quality.
US7915237 Production of pure stereoisomers of tricyclo[5.2.1.02.6]-dec-9-yl-xanthogenate and medicaments therefrom The invention relates to pharmaceutical formulations containing exo/exo-tricyclo[5.2.1.02.6]-dec-9-yl-xanthogenate, drugs containing exo/exo-tricyclo[5.2.1.02.6]-dec-9-yl-xanthogenate as active ingredient for the treatment of genital herpes, labial herpes, AIDS, tumors or autoimmune diseases, and methods for the production of pure stereoisomers of tricyclo[5.2.1.02.6]-decan-9-ol and tricyclo[5.2.1.02.6]-dec-9-yl-xanthogenate.
US8470808 Oxidant scavengers for treatment of type I diabetes or type II diabetes The present invention relates, in one embodiment, to a method of preventing or treating diabetes using low molecular weight antioxidants. In a further embodiment, the invention relates to a method of protecting and/or enhancing viability of cells/tissues/organs during isolation (harvesting), preservation, expansion and/or transplantation. In yet another embodiment, the present invention relates to a method of inducing immune tolerance. The invention also relates to compounds and compositions suitable for use in such methods.
US20080003268 Unit serving appetite suppressant compositions with steroidal glycosides An inherently nourishing edible appetite suppressant unit serving product comprising a steroidal glycoside, preferably obtainable from Hoodia plants, in a defined proportion to the total energy content. A method of lowering daily calorie (daily energy) intake is also disclosed.
WO2007122970A1 Ligand capable of binding to nuclear receptor Disclosed is a peroxisome proliferator-activated receptor gamma (PPARϜ) agonist which comprises a compound represented by the general formula (I) or a salt thereof or a prodrug of the compound or the salt: (I) wherein the ring A represents a heterocyclic ring; R1 represents a hydrogen atom or a carboxyalkyl group which may be esterified; R2 represents -COR5 (wherein R5 represents a C6-14 aryl group which may have a substituent or a heterocyclic group which may have a substituent) or -NO2; R3 represents a hydrogen atom, a halogen atom or a carboxyl group which may be esterified; and R4 represents a hydrogen atom or a C1-6 alkyl group.
US20080021004 Sapogenin derivatives and their use in the treatment of cognitive dysfunction The invention discloses the use of sapogenin derivatives in the treatment of cognitive dysfunction and similar conditions. Methods of treatment and pharmaceutical composition are also disclosed.
EP2265587A1 Modulators of the histamine h3 receptor useful for the treatment of disorders related thereto Amide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as excessive daytime sleepiness, narcolepsy, shift-work sleep disorder, drowsiness as a side effect from a medication, maintenance of vigilance to aid in the completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.
WO2014053579A1 A combination of adrenalin with an antidepressant for use in the treatment of shocks The present invention concerns a novel combination of adrenalin with an antidepressant and its use as a pharmaceutical composition for the treatment of shocks. The pharmaceutical composition is to be administered by injection.
CN103655530A Rapidly dispersed terbinafine hydrochloride medicament composition The invention discloses a rapidly dispersed terbinafine hydrochloride medicament composition. According to a formula of the medicament composition, formula selection finds by accident that sodium lauryl sulfate can effectively prompt terbinafine hydrochloride to rapidly disintegrate and effectively inhibit increase of relevant substances; the terbinafine hydrochloride medicament composition is good in stability, so that the product disclosed by the invention is high in yield, low in cost and easy for industrial production, can be well applied to clinical treatment, and has remarkable advantages.
CN103638314A Medicament for treating thyroid adenoma and preparation method of medicament The invention discloses a medicament for treating thyroid adenoma and a preparation method of the medicament. The medicament is mainly prepared from medicines such as artemisia anomala, dutchmanspipe root, bryozoatum, oyster, rhizoma polygonati, Paris polyphylla, concha arcae, radix semiaquilegiae, dicliptera chinensis, blackberry lily, pastinaca sativa, jellyfish and the like according to a certain weight ratio. The medicament disclosed by the invention has the functions of clearing away heat and toxic materials, relieving swelling and pain and activating blood to restore menstrual flow, and is rapid to take an effect and good in curative effect when used for treating thyroid adenoma, and the disease is not easy to reoccur after being healed.
US20080095834 Mitochondriotropic Phospholipid Vesicles Mitochondriotropic phospholipid vesicles, i.e., mitochondriotropic liposomes, that comprise a hydrophobized amphiphilic delocalized cation, such as those comprising, e.g., a triphenylphosphonium or a quinolinium moiety, incorporated into the phospholipid membrane of the vesicles, or liposomes, are disclosed. The hydrophobized portion of the amphiphilic delocalized cation, e.g., a fatty acid or other phospholipid derivative, is embedded in the phospholipid membrane of the liposome, and the amphiphilic portion of the cation is exposed on the surface of the liposome. Mitochondriotropic liposomes constitute a mitochondria-targeted drug delivery system, permitting the transport of a high payload of therapeutic water-soluble molecules in their native (i.e., active) state specifically and exclusively to mitochondria in living mammalian cells.
CN101250175A Preparation of myricetin, medicinal preparation and new medical usage The invention discloses a method for industrially preparing myricetin from Chinese ampelopsis or other vitaceae Chinese ampelopsis plant, a myricetin drug and a new medical application. The preparation method comprises using calcium oxide or calcium hydroxide to adjust water solution, hydrous ethanol solution or hydrous methanol solution to alkali, extracting the total flavonoids from medicinal materials, concentrating extract, adjusting pH value via dilute acid to 2-8 and crystallizing, to obtain crude extract, heating and extracting the crude extract via ethanol, methanol and acetone, and crystallizing to obtain myricetin. The method has simple process, low cost, non pollution, advanced property, safety and suitability. The medical application is the preparation of the drug for preparing and treating gynecologic diseases as pelvic inflammation, annexitis, cervicities and vaginitis or the like, while the drug can only contain myricetin or relative composite, and can be tablet, capsule, granules, dropping pill or injection or the like.
US7884082 Combined therapeutical treatment of hyperproliferative diseases A medicinal combination of one or more nucleic acids that at least partially inhibit oncogenic cell signalling pathways, and a therapeutic anticancer agent, for use simultaneous, separate or over a period of time to treat hyperproliferative diseases.
US20100298297 Tetrahydropyridothienopyrimidine Compounds and Methods of Use Thereof This invention relates to compounds of Formula (I), wherein the variables are as disclosed in the specification, to pharmaceutical compositions containing them, to methods of making the compounds and pharmaceutical compositions, and to methods of using the compounds and pharmaceutical compositions for treating or preventing disorders, in particular cancer.
CN103391775A Use of the phytocannabinoid cannabidiol (cbd) in combination with a standard anti-epileptic drug (saed) in the treatment of epilepsy The invention relates to the use of cannabidiol (CBD), at a dose of greater than 300mg/day, in combination with a standard anti-epileptic drug (SAED) which acts via sodium or calcium channels,for use in the treatment of epilepsy.The SAED is preferably one which DEG modifies low-threshold or transient neuronal calcium currents,or DEG reduces high-frequency neuronal firing and sodium-dependent action potentials and enhances GABA effects. Preferred SAEDs are ethosuximide and valproate.
US20050107353 Methods of treating lower urinary tract disorders using losigamone The invention relates to methods of using sodium channel modulators, preferably Losigamone or a pharmaceutically acceptable salt, enantiomer, analog, ester, amide, prodrug, metabolite, or derivative thereof, to treat painful and non-painful lower urinary tract disorders, particularly painful and non-painful overactive bladder with and/or without loss of urine.
CN101554411A Method for dispensing prescription for treating burn and scald The invention discloses a method for dispensing prescriptions for treating burn and scald; the medicine features easy configuration, low cost, convenient use, good curative effect, short course of treatment and no scar; the medicine is dispensed by the following materials by weight ratio: 200-300g of skullcap, 400-600g of mink oil, 200-300g of white granulated sugar and 200-300g of rhubarb; the dispensing method has the following steps: 1. weighing skullcap according to the weight ratio, decocting the skullcap in water, deslagging the mixture and getting water for standby use; 2 weighing fresh mink oil and putting the mink oil in a container to fry for obtaining the oil, slagging the oil for standby use; 3 putting 1000-1500g of clean water in a container and boiling the water, then adding white granulated sugar to water following the weight ratio, stirring the mixture; adding rhubarb according to the weight ratio for boiling decocting for 5min and stopping heating; adding the decocted skullcap water and the fried mink oil for standby into the mixture, then cooling the mixture, thus obtaining the medicine for treating burn and scale.
WO2010054058A1 Imidazolothiazole compounds as modulators of protein kinase Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
CN101032525A Extracting active principles having extracorporeal anti-tumor function from housefly larva The present invention relates to one kind of antitumor compound for inhibiting the proliferation of human cancer cell. The antitumor compound is unsaturated fatty acid extracted and separated from foreign matter induced maggot. Experiment shows that the antitumor compound has obvious inhibiting effect on the proliferation of human myelocytic leukemia HL-60 cell and human lung adenocarcinoma A549 cell, much higher than that of corresponding maggot powder, and no toxicity.
WO2012129765A1 Method for preparing stable-type vitamin a microcapsules continuously A method for continuously preparing stable-type vitamin A microcapsules is disclosed. The method comprises the following steps: adding vitamin A crystals and an antioxidant into a crystal melter continuously according to a certain ratio under the protection of nitrogen to prepare vitamin A melting oil containing the antioxidant; pumping the above melting oil into a high gravity rotary packed bed emulsifier with a liquid distributor by a pump, and pumping aqueous solution containing gellable modified starch into the above high gravity rotary packed bed emulsifier after deoxidation treatment to obtain vitamin A emulsion at the outlet of the high gravity rotary packed bed emulsifier; and atomizing and spraying the emulsion continuously in a cooled starch bed for granulating, and performing fluidization drying and gelation treatment in a fluidized bed by taking nitrogen as a drying medium to obtain the stable-type vitamin A microcapsules. Above method has the advantage of capability of continuous production, and has good embedding effect due to adopting the gellable modified starch, granulating and gelation treatment, thus the product has good storage stability.
US6921823 1,2,3,4,5,6-Hexahydroazepino[4,5-b]indoles containing arylsulfones at the 9-position The present invention are substituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (X) and unsubstituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (XI) such as the compound of EXAMPLE 13 which are useful in treating depression, obesity and other CNS disorders.
WO2011123945A1 Compostions, methods and uses for treating respiratory syncytial virus infection Provided herein is a method of treating Respiratory Syncytial Virus (RSV) infection in a cell. The method involves administering a nucleolin peptide, a nucleotide antibody, or a nucleolin RNAi to the cell.
US20100280060 Methods of screening and compositions for life span modulators Identification of nucleic acids involved in life span diseases and disorders or related diseases and disorders, and the use of such methods for identifying candidate agents which modulate life span diseases and disorders or related diseases and disorders are provided. Compositions and methods for treating life span diseases and disorders or related diseases and disorders are provided. Pharmaceutical compositions for treating life span diseases and disorders or related diseases and disorders are also provided
WO2013129929A1 Methods for activating retrovirus in latent infected cells, and compounds for use therein The present invention relates to a method for increasing retrovirus transcription in an infected eukaryotic cell, comprising increasing Wnt pathway signaling in said cell such that transcription of said retrovirus is increased. Also, the present invention relates to a method of treating a subject infected with a retrovirus, said method comprising administering to said subject an activator of the Wnt pathway in an amount that increased Wnt pathway signaling in resting memory CD4+ T cells of said subject such that the retroviral long terminal repeat (LTR) in said cells is activated or de-repressed.
WO2010053861A3 Biologically active amides The present invention is directed to biologically active amides which are ligands at the NPY Y5 receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from certain disorders which comprises administering to the subject an amount of a compound of the subject invention. Furthermore, this invention also provides uses of a compound of the invention for the manufacture of a medicament for treating a subject suffering from certain disorders.
WO2006093337A1 Preventive/therapeutic agent for cancer It is intended to identify a novel preventive/therapeutic target molecule of cancer and to provide a preventive/therapeutic agent for cancer that targets the molecule, in other words, a cancer cell apoptosis promoter and/or cancer cell growth inhibitor and a preventive/therapeutic agent for cancer containing an antibody against a protein having an amino acid sequence identical to or substantially identical to an amino acid sequence represented by SEQ ID NO: 2, SEQ ID NO: 4, SEQ ID NO: 6, SEQ ID NO: 8 or SEQ ID NO: 10, an antisense polynucleotide of the protein (preferably an siRNA against mRNA of the protein), or a substance that regulates the expression and/or activity of the protein. Further, it is intended to provide a method for screening a cell apoptosis promoting substance and/or cell growth inhibiting substance or a preventive/therapeutic substance for cancer utilizing the protein (preferably a cell producing the protein) and an antibody against the protein, or a polynucleotide encoding the protein.
CN103251716A Swelling-diminishing pain-erasing ointment and preparation method thereof The invention belongs to the medical field, in particular relates to swelling-diminishing pain-erasing ointment and a preparation method thereof, and aims at lowering the production period of the swelling-diminishing pain-erasing ointment. The swelling-diminishing pain-erasing ointment comprises the following bulk pharmaceutical chemicals: ligusticum wallichii, Chinese angelica, madder, green tangerine peel, red flower, ephedra and borneol. The swelling-diminishing pain-erasing ointment is prepared by the following method: A, crushing the drugs into crude powder except borneol, extracting by using 60%-80% of alcohol, and filtering to obtain filtrate; B, recycling the alcohol and concentrating the recycled alcohol to obtain thick ointment with relative density of 1.3-1.34 (at 80 DEG C); C, taking and uniformly mixing BC-1 medical pressure sensitive adhesive with trichloromethane in a weight ratio of 1:1 to form substrate; and D, uniformly stirring the thick ointment with the substrate in the weight ratio of 1:2, adding borneol for uniformly mixing, filtering to obtain paint, coating the ointment, drying, slitting, bushing and slicing to obtain the swelling-diminishing pain-erasing ointment. According to the swelling-diminishing pain-erasing ointment and the preparation method thereof, trichloromethane is used for dissolving the BC-1 medical pressure sensitive adhesive, so that the production period can be remarkably shortened, and therefore, the ointment surface appearance is more beautiful, the viscosity is properly lowered, and a patient can use the ointment more comfortably.
CN103360305A Substituted aryl piperazine aralkyl ketone derivative and application of derivative in preparing analgesic The invention discloses a substituted aryl piperazine aralkyl ketone derivative and an application of the derivative in preparing an analgesic. The substituted aryl piperazine aralkyl ketone derivative as well as physiologically acceptable salt thereof have quite a useful pharmaceutical property and excellent tolerance, particularly applied as a novel analgesic. The compound is a non-addictive central analgesic and free from remarkable sedation through animal experiments, and the compound is quite low in toxic and side effects and relatively high in a safety index. The substituted aryl piperazine aralkyl ketone derivative is free alkali or salt of a compound expressed as the structural general formula in the specification.
CN101104615A Anticancer cytoskeleton inhibiting and cell elongation inducing compound and synthetic method thereof The present invention discloses an anti-cancer cytoskeleton restraint and cell elongation attraction compound and the synthesis method, wherein, the compound is 7-chloro-6-piperidin-1-yl-quinoline-5, 8-dione (chemical name: 7-chloro-6-piperidin-1-yl-quinoline-5, 8-dione), and the chemical formula of the compound is C14H13ClN2O2, which is known as PT-262 in shortened form. The compound can stabilize actin filament to enable abnormal polymerization of actin filament, resulting in cancer cell elongation. In addition, PT-262 is provided with antitumor activity, which can block the survival path of Ras-ERK protein in cancer cells to result in cancer cell apoptosis, destroy mitochondrial membrane and accelerate the activation of caspase-3 protein. Moreover, PT-262 can inhibit the content of cyclic protein B1 and phosphorylation cdc2 protein (phospho-cdc2) to bring on the cessation of cancer cell cycle stop and inhibit the growth of cancer cells.
WO2012048013A3 Phosphorodiamidate derivatives of guanosine nucleoside compounds for treatment of viral injections This invention is directed to novel compounds of formula (I) having the structure that are useful in the treatment of viral infections in mammals mediated, at least in part, by a virus in the Flaviviridae family of viruses. Methods of treating viral infections via administration of these compounds are also disclosed.
CN102056930A Halichondrin B analogs The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediates.
CN101104591A Polymorph of proparacaine hydrochloride and preparation method thereof The invention relates to polymorphs and the making method of Proparacaine Hydrochloride (the chemical name is 3-amido-4 p propyl aminobenzoic acid-2-(ethylamino) ethyl ester mono hydrochloride). Two polymorphs of Proparacaine Hydrochloride can be obtained by choosing different solvent and different temperatures.
WO2012141796A3 Prostate cancer therapy with hsp90 inhibitory compounds Method for treating a subject with prostate cancer, comprising administering to the an effective amount of a compound represented by the following structural formula: a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein.
CN103505404A Oral liquid preparation with roxithromycin as active component The invention discloses an oral liquid preparation with roxithromycin as an active component. The oral liquid preparation is characterized by comprising the roxithromycin, stabilizing agent, solubilizer, pH regulating agent, flavoring agent and water. The oral liquid preparation has active advanced effects of preparing the unstable roxithromycin into the oral liquid preparation, ensuring the bioavailability consistency, largely reducing the risk in clinical application and guaranteeing the clinical effects.
CN103393668A Application of Sarcaboside B to medicament for treatment of pancreas cancer The invention discloses application of Sarcaboside B to preparation of medicaments for treatment of pancreas cancer and belongs to the technical field of novel application of medicaments. Through in vitro MTT antineoplastic activity evaluation, it is discovered that Sarcaboside B has substantial inhibition effect on growth of human pancreas cancer cell strains PANC-1 and BXPC-3. Accordingly, the Sarcaboside B can be applied to the preparation of medicaments for resisting pancreas cancer and has good development and application prospects. The application of Sarcaboside B to preparation of medicaments for treatment of pancreas cancer involved in the invention is disclosed for the first time. The Sarcaboside B has a novel skeleton type and unimaginably strong activity in inhibition of pancreas cancer cells.
EP2363128A2 Indole modulators of ATP-binding cassette transporters The present invention relates to modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ("CFTR"), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
US20100111917 Cell-adhesive polyelectrolyte material for use as membrane and coating A multilayer polyelectrolyte support material is provided that includes a polyelectrolyte layer and a polyelectrolyte-polyethylene glycol layer adjacent to the polyelectrolyte layer. The support material also includes a ligand conjugated to the polyelectrolyte-polyethylene glycol layer, allowing for attachment of a protein or a cell to the support material with controlled orientation.
CA2246430C Protein tyrosine phosphatases of hematopoietic cells This invention concerns new non-receptor protein tyrosine phosphatases of the hematopoietic stem cells (PTP HSC). The invention specifically concerns native murine and human PTP HSCs, their analogs in other mammals, and their functional derivatives. The invention further relates to nucleic acid encoding these proteins, vectors containing and capable of expressing such nucleic acid, and recombinant host cells transformed with such nucleic acid. Assays for identifying agonists and antagonists of the native PTP HSCs, methods for expansion of undifferentiated stem cells, and methods for the induction of stem cell differentiation are also within the scope of the invention.
US20080261915 Wound-Healing Pharmaceutical Compositions in the Form of a Sterile Powder Based on Amino Acids and Sodium Hyaluronate This invention relates to wound-healing pharmaceutical compositions in the form of a sterile powder based on amino acids and sodium hyaluronate.
US20110034926 Bioresorbable material The present invention in a first aspect relates to an element having a nonporous hollow body and a filling, wherein the nonporous hollow body is formed from bioresorbable magnesium and/or a bioresorbable magnesium alloy and the filling comprises a biocomposite material, wherein the biocomposite material comprises at least one biocompatible polymer component A and one ceramic component B. In a further aspect, the present invention is directed to a method for producing this element, which is especially suitable for use in bone surgery.
US20110021617 Medicinal Acidic Cannabinoids The invention relates to an acidic cannabinoid for medical use and to a cannabis extract comprising an acidic cannabinoid. The extract may comprise one or more compounds selected from the group consisting of cannabidiolic acid (CBD-A), cannabidiol (CBD), cannabigerolic acid (CBGA), cannabigerol (CBG), cannabinolic acid (CBN-A) and cannabinol. The invention further relates to a method for preparing a preparation comprising extracting an acidic cannabinoid from cannabis.
EP2603223A1 Recombinant tumor vaccine and method of producing such vaccine The present disclosure provides tumor vaccines useful for preventing and treating tumors and cancers. The tumor vaccines may contain nucleic acids encoding for antigen presenting peptides, cytokines and other factors useful for preventing and treating tumors and cancers, or expression vectors or viruses containing such nucleic acids, or host cells containing such nucleic acids or expression vectors.
CN103705502A Application of flavonoid compound in treating inflammatory diseases The invention discloses application of flavonoid compound 5,7,3',4',5'-pentamethyl flavanone (PMFA) as an active ingredient for treating inflammatory diseases. The 5,7,3',4',5'-pentamethyl flavanone (PMFA) taken as an anti-inflammatory active ingredient has the characteristics of small toxicity and good treatment effect, and has an obvious inhibitory effect on inflammatory factors and especially macrophage cytokines. Thus, the 5,7,3',4',5'-pentamethyl flavanone (PMFA) can be taken as an anti-inflammatory preparation used for the inflammatory diseases in which other various macrophage cytokines are participated such as sepsis, arthritis, immune-type enteritis, diabetes and the like, and especially has a good treatment effect on the sepsis which is difficult to cure.
CN102144969A Method for preparing etoposide nanometer suspension freeze-drying preparation The invention relates to a method for preparing an etoposide nanometer suspension freeze-drying preparation, and belongs to the technical field of medicines. An etoposide nanometer suspension of which the grain diameter is less than 200 nanometers is prepared by a high-pressure homogenization technology, and the suspension is filtered, sterilized and freeze-dried to form solid powder. By the preparation method, a large amount of cosolvent and surfactant which are used in the conventional etoposide injection can be prevented, so that the incidence rate of toxic and side reactions is reduced, and the stability of the preparation is improved; and albumin used in the preparation method can be used as a cryoprotectant, so other auxiliary materials are prevented from being added. The preparation method is easy to operate, mild in conditions and high in controllability and suitable for industrial production; and the prepared etoposide nanometer suspension freeze-drying preparation has the advantages of high safety and stability, low toxic and side effect and the like.
US20120157392 Epilepsy treatment employing ketogenic compounds which arrest apoptosis Method of treating a patient suffering from apoptosis of tissue by administering to the patient a therapeutically effective amount of one or more ketogenic compounds such that a physiological ketosis is produced which arrests the apoptosis.
CN103494841A Burn and scald liquid enabling scar not to be left and preparation method thereof The invention mainly relates to burn and scald liquid enabling a scar not to be left. The burn and scald liquid enabling the scar not to be left comprises, by weight, 20-40 parts of egg white, 0.1-4 parts of calomel, 0.2-1.2 parts of rifampicin, 40-60 parts of ethyl alcohol and 200-300 parts of distilled water, wherein the mass concentration of the ethyl alcohol is larger than or equal to 50%. The burn and scald liquid enabling the scar not to be left is suitable for various burns and scalds, such as a lime burn, a powder burn, an electric burn and a boiling water burn. After a person is burned, the burn and scald liquid is instantly prepared and applied. The burn and scald liquid is capable of producing the instant analgesia and detumescence effects and diminishing inflammation of the surface, remarkable in granulation promoting and inflammation diminishing effect, and capable of enabling the recovery speed to be high and enabling the scar not to be left after recovery. The burn and scald liquid is suitable for being used instantly after the person is burned or scalded, if other medicine is applied firstly, the burn and scald liquid can replace other medicine, and the burn and scald liquid produces an instant effect after being applied, and can reduce the possibility of appearance of the scar.
WO2007147770A3 Substituted phenyl methanone derivatives The present invention relates to compounds of the general formula (i), wherein R1 is -OR1', heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by lower alkyl or halogen; R1' is lower alkyl, lower alkyl substituted by halogen, or is -(CH2)o-cycloalkyl; R2 is -S(O)2-lower alkyl, -S(O)2NH-lower alkyl, NO2 or CN; R3 is aryl or heteroaryl, which are unsubstituted or substituted by one to three substituents, selected from the group consisting of lower alkyl, lower alkoxy, CN, NO2, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, aryl or sulfonamide; X is a bond, -CH2-, -NH-, -CH2O- or -OCH2-; n is 1 or 2; m is 1 or 2; o is 0 or 1; to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them and their use in the treatment of neurological and neuropsychiatric disorders. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1).
US20090062312 Deuterium-enriched indiplon The present application describes deuterium-enriched indiplon, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2009071691A3 Oxindole derivatives and the use thereof as a medication The present invention relates to novel substituted oxindole derivatives of formula (I), pharmaceutical agents containing them, and the use thereof for the treatment of vasopressin-dependent illnesses.
CN102068411A Carbazole sulfonamide type anti-tumor medicament granules and preparation method thereof The invention belongs to the field of medicament preparations and relates to a preparation method of an anti-tumor preparation, in particular to carbazole sulfonamide type anti-tumor medicament granules and the preparation method thereof, and the preparation method is characterized in that lactose and beta-cyclodextrin are added in a carbazole sulfonamide type medicament which is N-(2,6-dimethoxy pyridine-3-substituted)-9-methylcarbazole-3-sulfonamide, the mixing is performed, the mixture is milled to micro-powder and prepared into granules, and the dissolution rate of the granules can be improved.
WO2014155144A1 Stable nanocomposition comprising docetaxel, process for the preparation thereof, its use and pharmaceutical compositions containing it A nanoparticulate composition is disclosed for the targeted therapeutic treatment of tumours. The stable self assembled nanocomposition according to the invention comprises (i) a carrier and targeting system comprising an optionally modified polyanion, and optionally a polycation, which may also be modified; at least one targeting agent which is linked to either the polycation/modified polycation or the polyanion/modified polyanion, or both or to the surface of the nanoparticle; (ii) an active compound selected from the group of docetaxel and its pharmaceutically acceptable salts and derivatives especially its hydrates, especially docetaxel trihydrate and docetaxel trihydrate monohydrochloride; and optionally (iii) at least one complexing agent, a metal ion and a stabilizer/formulating agent, or a PEGylating agent. The present invention furthermore relates to a process for the preparation of the above-mentioned composition, the therapeutic uses thereof, and pharmaceutical compositions containing the nanocomposition according to the invention.˙
WO2008111384A1 Epithelium improving agent It is intended to provide an epithelium improving agent which improves the epithelial functions of various organs and, therefore, is usable in growing melanin-pigmented hair, relieving inflammatory symptoms in gingivitis and paradentitis, treating and relieving cold syndrome and bronchial asthma and, moreover, restoring sexual sensibility. An epithelium improving agent which comprises coenzyme Q10, cysteine, vitamins A, C and E and a skin extract of a rabbit inoculated with a vaccinia virus as the main components. In the case of treating gingivitis, paradentitis, cold syndrome and bronchial asthma, loratadine is further added. To an epithelium improving agent which is to be used in stimulating hair growth or restoring sexual sensibility, liquid paraffin and a hydrophilic ointment is further added to give a cream. Thus, the above problem can be solved.
US20100311814 Modulation of stat5 expression Compounds, compositions and methods are provided for modulating the expression of STAT5. The compositions comprise oligonucleotides, targeted to nucleic acid encoding STAT5. Methods of using these compounds for modulation of STAT5 expression and for diagnosis and treatment of diseases and conditions associated with expression of STAT5 are provided.
WO2014063596A1 Oral formulation for treating diabetes An oral formulation, preparation method therefor and use thereof. The oral formulation comprises a pharmaceutically acceptable carrier and 17α-ethynyl-androst-5-ene-3β, 7β, 17β-triol as active ingredient; the formulation is not released or is substantially not released in an acidic medium.
CN101284096A Sheep placenta capsule compound nest-defence capsule for beautifying face The invention belongs to the technology field of Tibetan medical health food, particularly a hard capsule prepared from saffron extract, Tibetan medlar extract, Tibetan solomonseal extract, Tibetan angelica extract, Chinese yam extract, multiflower knotweed root extract, seaweed extract, proanthocyanidin , vitamin B6, vitamin E, vitamin C, etc. The prepration process for the hard capsule includes mixing the materials, stirring; filling into capsules, sealing; checking; and packaging to obtain finished product. The capsule is effective in caring ovary, caring skin, postponing aging, etc.
WO2011158176A3 Gold complexes for use in the treatment of cancer The invention provides compounds of the Formula (I), in which W is independently selected from W1, W2, W3, W4, W5, or W represents a pair of substituents independently selected from H, alkyl, aryl or amide in which the amide is optionally part of a linking chain, and the Zn-Zn bonds (n = 4-17; n' = n + 1 ) are optionally of any whole or partial bond order, Y is Y1 or Y represents a pair of substituents independently selected from H, C-1-C6 alkyl, Z5 or Z6 aryl, or Y is optionally a bridging structure that may comprise one or more C-1-C6 amide, C-1-C6 ether, or C-1-C6 ester groups, R-R39 are independently selected from no substituent, a lone pair of electrons, H, halogen, C5-C6 aryl, C1- C-12 alkyl, amine, C-1-C6 alkylamine, C-1-C6 amide, nitro, cyano, carboxyl, C-1-C6 ester, phosphane, thiol, C-1-C6 thioether, OR40, and suitable pairs of adjacent R groups (R-R39) may optionally together form part of a C5 or C6 aryl ring, a Z5 or Z6 ring, R40 is independently selected from H, C-1-C6 alkyl, Z5 or Z6 aryl, C-1-C6 ester, poly(-C2O-), amine, and C-1-C6 alkylamine, Z-Z24 are independently selected from C, N, P, O, and S, and X- is a pharmaceutically acceptable anion, for the treatment of cancer.
WO2013167743A1 Use of compounds for the treatment of pain The present invention relates to new therapies to treat pain and related diseases, as well as pharmaceutical compounds for use in said therapies.
US6956053 Mixtures of gastric juice secretion antagonist and proton pump inhibitors used for prophylaxis of eating disorders; cyclization Compounds of formula (I), (IIa) or (IIb) wherein R1-R6, Z, Q and n are as defined in claim 1 and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. Compositions comprising a compound of formula (I), (IIa) or (IIb) are also described.
EP2616470A1 Purine compounds as prodrugs of a2b adenosine receptor antagonists, their process and medicinal applications The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists. {Formulas should be inserted here} The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. Such conditions include, but are not limited to, asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders including inflammatory bowel disease, sickle cell disease, and/or autoimmune diseases. and to their use in treating mammals for various disease states, such as gastrointestinal disorders, immunological disorders, hypersensitivity disorders, neurological disorders, and cardiovascular diseases due to both cellular hyperproliferation and apoptosis, and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
US20130064904 Preparation and compositions of highly bioavailable zerovalent sulfur and uses thereof The present invention features sulfur-rich compositions and preparations thereof that are safe and effective as hydrogen sulfide prodrugs of high bioavailability. The invention also includes methods of treating pathological conditions associated with oxidative stress using sulfur-rich compositions. The invention further includes sulfur-rich compositions as antidotes and medical food for preserving and promoting general health.
EP1280528B1 R-eliprodil for treating glaucoma Methods for treating glaucoma with R-eliprodil alone and in combination with other agents for treating glaucoma are disclosed.
US20100003236 Use of c-glycoside derivatives as pro-desquamating active agents A cosmetic use of at least one C-glycoside derivative in a composition comprising a physiologically acceptable medium, as a cosmetic agent for promoting the desquamation of the skin and/or the scalp and/or for stimulating epidermal renewal.
US20100210627 Pyrazine compounds, their use and methods of preparation The invention provides compounds according to formula (I) their use and methods for preparation wherein A, X, Y, R1, R2 and R3 are defined herein. The compounds of the invention inhibit specific serine/threonine kinases involved in inflammatory processes and aberrant cell proliferation, and are thus useful for treating associated diseases and pathological conditions such as Pim kinase-mediated diseases and pathological conditions involving inflammation, including Chron's disease, inflammatory bowel disease, rheumatoid arthritis, and chronic inflammatory disease, or aberrant cell proliferation including various cancers.
US20090062375 Methods and compositions for the treatment of viral diseases The invention provides a method of treating viral haemorrhagic fevers, such as that caused by Dengue virus, which comprises administering a composition comprising a pharmaceutically active amount of a matrix metalloproteinase inhibitor.
WO2008155520A2 4-hydroxy benzoate derivatives for use in the treatment of infection, inflammation or pain The invention provides a compound of the general formula (I) for use in the topical treatment of infection, inflammation and/or pain: wherein R1 independently represents a methylene group, an ethylene group or a straight or branched chain C3 to C6 alkylene group; R2 independently represents a hydrogen atom, a methyl group, an ethyl group or a straight or branched chain C3 to C20 alkyl group; x represents 0 or an integer from 1 to 4 and y represents 0 or an integer from 1 to 4, wherein the sum of x and y is 4; and Z represents a hydrogen atom or (HOR1)yR2XN⊕; compositions comprising the compound; use of the compound in the manufacture of a medicament; and methods of medical treatment comprising the topical application of the compound.
EP2690096A1 Process for preparation of Bendamustine The present invention relates to a method for preparation of alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7) from 2-fluoro-5-nitroaniline, comprising the steps of: a) conversion of 2-fluoro-5-nitroaniline to 5-(2-fluoro-5-nitroanilino)-5-oxopentanoic acid (1) using glutaric anhydride, conversion of compound (1) to methylammonium 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoate (2) using methylamine; conversion of compound (2) to 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoic acid (3) and condensation of compound (3) to 4-(1-methyl-5-nitro-1H-benzimidazol-2-yl)butanoic acid (4), b) esterification of the product (4) of step a) to alkyl 4-(1-methyl-5-nitro1H-benzimidazol-2-yl)butanoate (5), c) reduction of the product of step b) to alkyl 4-(5-amino-1-methyl-1H-benzimidazol-2-yl)butanoate (6), and d) conversion of the product of step c) to alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7).
EP1593678A1 Crystal of (23s)-1alpha-hydroxy-27-nor-25-methylenevitamin d3-26,23-lactone and process for producing the same A crystal of (23S)-1α-hydroxy-27-nor-25-methylenevitamin D3-26,23-lactone described in the following formula is provided which shows a specific powder X-ray diffraction pattern or a specific infrared spectroscopic pattern.
CN103566008A Saururus chinensis extract as well as preparation method and application thereof The invention provides a novel application of saururus chinensis extract in preparation of medicine for preventing Epstein-Barr (EB) virus infection and also provides five novel compositions and a preparation method of the saururus chinensis extract. The saururus Chinensis extract has good treatment capability for the EB virus infection, is low in toxicity and side effect and is an effective drug.
CN102302640A Blood-activating and pain-relieving plaster, and preparation method thereof The invention relates to a blood-activating and pain-relieving plaster, and a preparation method thereof. A formulation of the plaster comprises: garter snake, snake slough, nux vomica, doubleteeth angelica root, rheum, gansui root, scorpion, rehmannia dride rhizome, asurum uropeum, zhishi, fructus crotonis, almond, divaricate saposhnikovia, kusnezoff monkshood root, angelica archang lica, nutgrass galingale rhizome, clam powder, frankincense, pollen, whole ginseng, whole angelica, myrrh, knoxia root, herba ephedrae, dragon's blood, large cenpitede and forest musk. The preparation method comprises the following steps: pouring sesame oil or perilla oil to a container, boiling the oil, then adding garter snake, snake slough, nux vomica, doubleteeth angelica root, rheum, gansui root, scorpion, then adding other herbs, adding the dragon's blood after 4-5 hours; carrying out decocting with mild fire after all the herbs are added to the container; placing the decocted medical solution in cold water filled in a container to carry out cooling until the solution is transformed into the black solid. According to the present invention, the plaster can be directly pasted on the affected part of the human body and is applicable for most people; the plaster has characteristics of no skin irritation, no toxic and side-effect, simple process, fast release rate, quick therapeutic effect; the plaster is applicable for treating snake bite, small area burn, scald and other surgical wounds, and has effects of blood activating and pain relieving.
CN102349925A Application of astragaloside in preparation of drugs for promoting epithelization in wound healing The invention relates to application of astragaloside in preparation of drugs for promoting epithelization in wound healing. The astragaloside can correct the inhibition effect on the proliferation and migration of keratinocyte under the condition of imitating and activating a classical Wnt signaling channel with lithium chloride, thus the astragaloside has promotion action on the epithelization stage in wound healing process and can be used for preparation of the drugs for treating chronic skin ulcer or other skin wound surfaces. The invention has the advantages that: the new application of the astragaloside in pharmacy is developed, and a new application field is developed; the astragaloside can promote the proliferation and migration of keratinocyte, namely accelerate the epithelization course in wound healing process, therefore, the astragaloside has the effect of promoting wound healing and an important clinical basis is provided for prevention and treatment of chronic skin ulcer; and the astragaloside has wide raw material sources, low price, s and broad industrial prospects, and the preparation process of the astragaloside is simple. The astragaloside is suitable for wide popularization and use.
WO2013034087A1 Doripenem hydrate crystal and preparation method therefor Disclosed are a doripenem hydrate crystal and preparation method therefor. The X-ray diffraction spectrogram of the crystal powder is basically as represented in figure 1, and the measured water content is 4.4 to 5.5%. The doripenem hydrate crystal of the present invention has high purity, low residual solvent, good stability, and application safety. Additionally, the preparation method for the doripenem hydrate crystal of the present invention has simple techniques and low preparation cost, and is suitable for industrial production.
CA2612469A1 Benzimidazole derivatives for treatment of inflammatory diseases Benzimidazole derivatives, methods of preparing the same and their pharmaceutical uses for the treatment of inflammatory diseases including COPD.
US20120183538 Sparc antisense compositions and uses thereof The invention provides SPARC antisense oligonucleotides and methods of their use in proliferative diseases such as cancer and hepatic fibrosis.
EP1972340A2 Method of preparing an aqueous meloxicam solution and the resulting aqueous solution A method of solubilizing a selective inhibitor active agent of cyclo-oxigenase-2 (COX-2), such as meloxicam, and a method of preparing an ophthalmic solution from the solubilized meloxicam for the treatment of distinct ocular affections are described. The invention also refers to an aqueous ophthalmic solution resulting from the aforementioned method, said ophthalmic solution being characterized by its safety, innocuousness and efficiency in the treatment of the patient. The new aqueous ophthalmic solution is characterized in that its pharmaceutical value is found in the use of a vehicle of easy access which not only permits the solubility of meloxicam, but which also favors a greater patient tolerance to the treatment of distinct affections of the eye and the patient's post-surgical recovery.
WO2011106858A1 Fast-dissolving solid pharmaceutical form for treating bacterial infections The present invention relates to solid pharmaceutical compositions that dissolve readily and stably which are capable of inhibiting or eliminating an infectious process caused by bacteria in warm-blooded animals and aquatic species such as, for example, fish and crustaceans. The invention describes the composition of antibiotic-containing formulations to be administered by various routes for treating bacterial infections in warm-blooded animals and aquatic animals. The formulation can be designed for human and animal use.
WO2009111893A1 Substituted pyrimidine compounds and their use as ifnar mediators The present application relates to substituted pyrimidine compounds of Formula I and their use as ligands for IFNAR. The application further relates to methods of treating or preventing diseases or disorders that benefit from the modulation of IFNAR by administering an IFNAR effective amount of said compounds of Formula (I) to a subject need thereof.
CA2371853C Heterocyclic benzenesulphonamide compounds as bradykinin antagonists The invention concerns compounds selected among the group consisting of (i) compounds of formula (I) wherein: Het1 represents a nitrogenous heterocycle with 5 apices, in particular imidazole, pyrazole, or triazole; Het2 represents a nitrogenous heterocycle with 4, 5 or 6 apices, selected among the heterocycles: (II) wherein R1 and R2 are defined as mentioned in the description; and (ii) their additive salts. The invention also concerns the method for preparing said compounds and their use in therapy, in particular for treating pathologies involving bradykinine. (see formula I) (see formula II)
US20080070851 Method for the extraction of pharmaceutically active products from spermatophyte plants, products thus obtained and their use in the medical field, in particular as substances with immunomodulating activity A method is described for the extraction of products having a pharmacological activity, in particular an immunomodulating activity, from spermatophyte plants. Said products, which are to be used in the pharmaceutical fields, consist of complex mixtures of compounds characterized by one or more stilbene groups, variously hydroxylated and/or glucosidated, and of compounds derived from said group by natural enzymatic biosynthetical processes (stilbenoids). The following compounds are preferred: T-Res, C-Res, glucosidated C-Res, ε-viniferine, H-gnetine, r-2-viniferine, r-viniferine, hopeaphenol, Ampelopepsin A and glucosidated T-Res.
US20080280896 Dipyrrole Compounds, Compositions, and Methods For Treating Cancer or Viral Diseases The present invention relates to novel Dipyrrole Compounds, compositions comprising a Dipyrrole Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Dipyrrole Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus. The invention also provides screening assays for compounds that can be used in combination with Dipyrrole Compounds for the treatment of cancer or neoplastic disease, inhibition of cancer cell growth, or treatment of viral infections.
CN101069690A Doxycyline Hyclate lipid gels and preparing method The present invention discloses a doxycycline hydrochloride liposome gel preparation. It is made up by uniformly mixing (by wt%) 20-80% of doxycycline hydrochloride liposome and 80-20% of gel matrix. The invented doxycycline hydrochloride liposome gel preparation can be used as local antibiotic medicine, and can effectively prolong action time of medine and can raise antibacterial effect of medicine.
US20090324545 Polymorphic forms of (s)-1-tetrahydrofuran-3-yl-3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)benzyl carbamate The present invention relates to polymorphic forms of (S)-tetrahydrofuran-3-yl 3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)benzylcarbamate, processes therein, pharmaceutical compositions thereof, and uses therewith.
WO2011030205A1 N-substituted benzenepropanamide or benzenepropenamide for use in the treatment of pain and inflammation Compounds for use in the treatment or prophylaxis of pain, including acute and chronic pain (e.g., nociceptive pain, neuropathic pain, headaches, migraine), represented by general formula (I), in which: the dotted line represents a single or a double bond; and R5 and R5' are independently -H, -OH or -OR6, where R6 is a linear or branched C1-C4 alkyl; X is -CH2O-,; Z is -CH2CH2O-CH(CH3)CH2O- or -CH2CH(CH3)O-; m is 1; and n is an integer of 1- 5. The compounds of the invention are also effective for reducing inflammation and may be used alone or in combination with other analgesics.
WO2007036711A1 BENZIMIDAZOLONES WHICH HAVE ACTIVITY AT Ml RECEPTOR Compounds of formula (I) and salts and solvates are provided: wherein R6 is selected from hydrogen, halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano, and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
EP2660240A1 Benzopyrone estrogen receptor regulator The present invention provides a kind of benzopyrone compounds having a structure of formula (I) and the pharmaceutically acceptable salts or prodrugs thereof, and the pharmaceutical compositions containing such compounds, which can be used to regulate the novel estrogen receptor ER-a36, and prevent and/or treat the related diseases mediated by the ER-a36 receptor, such as cancers, etc.
WO2007126886A1 Process for preparing memantine hydrochloride substantially free of impurities The present invention encompasses processes for preparing Memantine hydrochloride and its derivatives, substantially free of impurities.
CN103539779A Hydroxyl substituted benzene sulfonate of dabigatran etexilate and preparation method and usage thereof The invention discloses a hydroxyl substituted benzene sulfonate of dabigatran etexilate and a preparation method and a usage thereof. The preparation method comprises: respectively adding dabigatran etexilate and hydroxyl substituted benzenesulfonic acid into an organic solvent, stirring and dissolving to obtain a clear solution; and reacting under a certain temperature, concentrating, stewing, separating out crystals, and filtering to obtain the hydroxyl substituted benzene sulfonate of dabigatran etexilate. The hydroxyl substituted benzene sulfonate of dabigatran etexilate provided by the invention has good stability; the provided preparation method is simple, convenient, feasible, stable and reliable, and a crystal form suitable for medicinal can be obtained; and the obtained product is good in quality and high in yield.
US8728511 Method of treatment comprising administering controlled release melatonin Controlled release melatonin formulations are useful for imparting avoidance of mood depression which may be associated with administration of melatonin in conventional form comprising. Particular embodiments of methods use formulations designed to release melatonin according to a profile that simulates a normal endogenous melatonin nocturnal profile. The methods also include co-administration with additional medicaments.
WO2014164784A1 Hdac inhibitor polymorphic forms and methods of use Polymorphic forms of histone deacetylase inhibitors (HDAC) and methods of making and using such polymorphic forms are provided. Crystalline polymorphic forms can be characterized by their X-ray powder diffraction patterns, solubility, stability and other properties.
US20110224292 Method and apparatus for determining anticoagulant therapy factors Methods and apparatus are disclosed for determining new anticoagulant therapy factors for monitoring oral anticoagulant therapy to help prevent excessive bleeding or deleterious blood clots that might otherwise occur before, during or after surgery. The inventive methods and apparatus provide an International Normalization Ratio (INR) based on a coagulation reaction with a blood sample of a living being. Embodiments include methods and apparatus for determining an anticoagulant therapy factor without requiring use of a mean normal prothrombin time determination or an ISI, and may be carried out with the patient sample and a coagulation reagent, where the coagulation reagent may be selected from a number of coagulation reagents. One embodiment provides an INRs value which is determined from a prothrombin time (PT or T1) of a patient blood sample and a theoretical end of test time (TEOT), where a theoretical clotting area is used to determine the INRs value according to the expression, INRs=T1*TEOT*MUL, where MUL is a multiplier that takes into account pixel parity and sampling times. The INRs may be used to determine a course of treatment for a patient or other living being without regard to the specific coagulation regent used to generate the coagulation data (e.g., time and optical activity values).
US20100099727 Amino acid and peptide conjugates of arylalkylic acids for cosmetic use The invention provides novel compounds of general formula I wherein R1, R2 and R3 are independently hydrogen, OR4, C1-C6 alkyl or C2-C6 alkenyl, R4 is hydrogen, C1-C6 alkyl or C2-C6 alkenyl, —N-(AA) represents the residue of an amino acid or of a peptide which is bonded over the N-terminus of the amino acid or the peptide and the peptide is composed of 2 to 6, that means 2, 3, 4, 5 or 6, amino acids, wherein the C-terminus of the amino acid or the peptide is optionally esterified with a C1-C16 hydrocarbon moiety and n is an integer of 1 to 5. The compounds are in particular useful for cosmetic applications.
WO2012150412A1 Novel combination of 4-(3-[cis-hexahydrocyclopenta[c]pyrrol-2(1h)-yl]propoxy)benzamide and an acetylcholinesterase inhibitor, and pharmaceutical compositions containing same The invention relates to a combination of the 4-(3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy)benzamide of formula (I), or of one of the addition salts thereof, with a pharmaceutically acceptable acid or base and an acetylcholinesterase inhibitor. The invention can be used in the field of drugs.
WO2010062372A2 Methods for modulating nf-kb using gibberellins The present invention provides methods for modulating the NF-κB pathway in a cell using gibberellins such as gibberellic acid. The invention also provides methods for using gibberellins in treating proliferative diseases (e.g., cancer), neurodegenerative diseases, autoimmune diseases, inflammatory diseases, and infectious diseases.
EP0758244B2 Controlled-release dosage forms of azithromycin A controlled-release dosage form of azithromycin having an improved side effect profile; a process for preparing the dosage form; and a method of treating a microbial infection, comprising administering azithromycin in such a controlled-release dosage form to a mammal, including a human patient, in need of such treatment.
US20090041716 Crystalline form of methyl ((1s)-1-(((2s)-2-(5-(4'-(2-((2s)-1((2s)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1h-imidazol-5-yl)-4-biphenylyl)-1h-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt The present disclosure generally relates to a crystalline form of methyl ((1S)-1-(((2S)-2-(5-(4′-(2-((2S)-1-((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1 H-imidazol-5-yl)-4-biphenylyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt. The present disclosure also generally relates to a pharmaceutical composition comprising a crystalline form, as well of methods of using a crystalline form in the treatment of Hepatitis C and methods for obtaining such crystalline form.
US20080194690 Pharmaceutical Formulations Of Hdac Inhibitors This invention pertains to pharmaceutical compositions comprising certain carbamic acid compounds (e.g., which inhibit HDAC (histone deacetylase) activity) (e.g., PXD-101, N hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide)) and one or more additional ingredients selected from cyclodextrin, arginine, and meglumine. The present invention also pertains to the use of such compositions, for example, in the inhibition of HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
US20090274687 Attenuation of hypoxia induced cardiovascular disorders Blockade of stromal derived factor-1 (SDF-1), a stem cell mobilizer and/or its receptor, chemokine receptor 4 (CXCR4) attenuates and reverses hypoxia-induced cardiopulmonary remodeling in vivo. Compositions for treating hypoxia-induced cardiovascular disorders modulate the SDF-1/CXCR4 axis.
EP1951222A2 Method of treating breast cancer using 17-aag or 17-ag or a prodrug of either in combination with a her2 inhibitor A method for treating a breast cancer in a subject by administering 17-allylamino-17-demethoxy-geldanamycin (17-AAG) or 17-amino-17-demethoxygeldanamycin (17-AG), or a prodrug of either 17-AAG or 17-AG, in combination with a HER2 inhibitor.
EP1944022A1 Pharmaceutical compositions combining analgesics and anticonvulsant agents for the treatment of chronic and acute pain The present invention relates to pharmaceutical industry in general, and to pharmaceutical industry making medicaments for treatment of conditions of sharp and chronic pain. The composition is characterized in that it comprises a combination of an analgesic and an anticonvulsant, wherein the analgesic is known as Tramadol and the anticonvu.lsant drug is known as Gabapentin, wherein Tramadol is present in a rate with respect to the total weight of the formulation of from 3 to 8.3% and Gabapentin is present in a rate with respect to the total weight of the formulation of from 16 to 83%.
EP1977749A1 Use of cyclooxygenase-2 inhibitors in the treatment and prevention of neoplasia The present invention relates to a pharmaceutical composition for the treatment of a neoplasia, which comprises a compound of formula II and an anti-neoplastic agent
US20100183705 Phospholipid-analogous compounds Phospholipid-analogous compounds of the general formula (I) in which A where R1 and R2 are, independently of one another, hydrogen, a saturated or unsaturated acyl or alkyl radical which can optionally be branched or/and substituted, where the total of the carbon atoms in the acyl and alkyl is 16 to 44 C atoms, s is an integer from 0 to 8, c is a radical of a primary or secondary alcohol of the formula RO—, where R is a saturated or unsaturated alkyl radical, mainly with cis double bond, of from 12 to 30 carbon atoms, n is an integer from 2 to 8, R3 a can be 1,2-dihydroxypropyl or b can be alkyl with 1 to 3 C atoms when z is >0 or c can be alkyl with 1 to 3 carbon atoms when n≠2 and z=0, m is 1 or 2, x is an integer from 0 to 8, y is 1 for z=1 to S′ or is 1 to 4 for z=1 z is an integer from 0 to 5, are novel and are suitable as liposome constituents, solubilizers and pharmaceuticals.
WO2004073619A3 Ccr8 antagonists This invention relates to certain substituted benzenesulfonamide and their use for inhibiting the chemokine receptor nominated CCR8. The generic structure for these compounds, as defined herein is that of a benzenesulfonamide of formula (I).
CA2474703C Therapeutic agent of glaucoma comprising bunazosin and prostaglandins It is intended to find out the usefulness of the combination of bunazosin with prostaglandins as remedies for glaucoma having a novel function mechanism. Namely, remedies for glaucoma comprising bunazosin or its salt together with prostaglandins. Bunazosin or its salt and prostaglandins supplement and/or potentiate the effects each other. It is possible to administer bunazosin or its salt together with prostaglandins in a single preparation, i.e., a combined drug. Alternatively, they may be administered separately, i.e., combined administration.
CN101496856A Proanthocyanidin chewing tablet The invention relates to a chewable tablet containing natural procyanidins. The chewable tablet contains grape pip extract, vitamin C, sodium vitamin C, taurine, sweetening agent, natural perfume, and one or more excipients. By supplementing natural oligomeric procyanidins, the chewable tablet can improve the radiation resisting capability and oxidation resisting capability of the human body, enhance eyesight, and keep the skin healthy.
CN101756983A Stable sitafloxacin medicine composition The invention relates to a stable sitafloxacin medicine composition, which comprises an effectively treatment amount of novel oral administration carbostyril antibiotic medicine selected from sitafloxacin, medicine stabilizing agents selected from sodium metabisulfite and the like and pharmaceutically acceptable accessory agents. The stable sitafloxacin medicine composition can effectively prevent the degradation of the effective ingredients, and can be used for treating single or mixed bacterial infection of the respiratory tract, the genitourinary tract, the abdominal cavity, the skin soft tissue and the like.
CN102166193A Phloretin pellet and preparation method thereof The invention relates to a preparation method of a phloretin pellet, which is simple, convenient and easy to operate. The preparation method overcomes the shortcomings in the prior art, and phloretin is prepared into a pellet type product with controllable release in the body and high bioavailability, so as to better meet the demands of general consumers. In the preparation method, the phloretin is ground into fine powder by adopting micronization technology, and the average particle size of the fine powder is generally less than 15 um and mainly distributed in the range of 5-20 um. By adopting the preparation method, the absorption rate of effective ingredients is increased, and the bioavailability is improved; and by adopting water-soluble adhesive and excipient, the solubility of the phloretin in the body is greatly enhanced, and as the solubility of the micron-sized effective ingredients in the gastrointestinal tract is significantly increased, the bioavailability of the micron-sized effective ingredients is increased, and the onset time of the micron-sized effective ingredients is shortened.
US20050032693 Novel polypeptides, their nucleic acids, and methods for their use in angiogenesis and vascularization The present invention is directed to novel polypeptides critical for angiogenesis and vascularization, and to nucleic acid molecules encoding those polypeptides. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Compositions and methods are disclosed for stimulating or inhibiting angiogenesis and/or neo- or cardio-vascularization in mammals, including humans. Pharmaceutical compositions are based on polypeptides or antagonists thereto that have been identified for one or more of these uses. Disorders that can be diagnosed, prevented, or treated by the compositions herein include trauma such as wounds; various cancers, and disorders of the vessels including atherosclerosis.
US20100233156 Treating Central Nervous System Injury with Beta and Gamma Secretase Inhibitors Provided herein are methods of treating an acute central nervous system injury in a subject. The methods comprise administering to the subject a γ or β secretase inhibitor, an Aβ antibody, or an immunogenic fragment of Aβ.
US20100190832 Mechanism-based inhibitors of transthyretin amyloidosis: studies with biphenyl ethers and structural templates Transthyretin (TTR), a tetrameric thyroxine (T4) carrier protein, is associated with a variety of amyloid diseases. Derivative of biphenyl ethers (BPE), which are shown to interact with a high affinity to its T4 binding site thereby preventing its aggregation and fibrillogenesis. They prevent fibrillogenesis by stabilizing the tetrameric ground state of transthyretin. Two compounds (2-(5-mercapto-[1,3,4]oxadiazol-2-yl)-phenol and 2,3,6-trichloro-N-(4H-[1,2,4]triazol-3-yl) exhibit the ability to arrest TTR amyloidosis. The dissociation constants for the binding of BPEs and compound 11 and 12 to TTR correlate with their efficacies of inhibiting amyloidosis. They also have the ability to inhibit the elongation of intermediate fibrils as well as show nearly complete (>90%) disruption of the preformed fibrils. Biphenyl ethers and compounds 11 and 12 as very potent inhibitors of TTR fibrillization and inducible cytotoxicity.
US20130045273 Methods for using nutritional supplements containing lipoic acids and sulfur containing compounds Methods for using nutritional supplements containing lipoic acids and sulfur containing compounds to maintain or increase the levels of cellular GSH in the body are described. In some instances, the nutritional supplements can increase both the levels of GSH, vitamin C, GST activity, and antioxidant protection in the blood. The nutritional supplement contain a first part containing an effective amount of a lipoic acid and a second part containing an effective amount of a sulfur containing compound that increases the level of GSH vitamin C, GST activity, and antioxidant protection in the blood The first part and second part of the nutritional supplement can be partially or completely separated. The increased GSH and vitamin C levels increases the detoxification ability of the body as measured by the GST (Glutathione S-Transferases) activity and the antioxidant protection as measured by SAR (Serum Antioxidant Reserve). Other embodiments are described.
CN102908399A A composition containing desert cistanche or cynomorium songaricum or medlar, lecithin and vitamin E The invention relates to the field of nutritious food, health food and medicine, and particularly relates to a composition capable of regulating blood lipids. The composition comprises the following components: 5-60 parts by weight of desert cistanche or cynomorium songaricum or medlar, 5-60 parts by weight of lecithin and 0.25-3 parts by weight of vitamin E.
US8703143 Antibodies of the ED-B domain of fibronectin, their construction and uses According to the present invention there is provided a specific binding member which is specific for and binds directly to the ED-B oncofoetal domain of fibronectin (FN). The invention also provides materials and methods for the production of such binding members.
CN103502275A Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same The present invention relates to the ability to regulate any protein of interest in living systems with small molecules. In particular, the present invention relates to the discovery that appending a hydrophobic moiety to the surface of a protein can mimic the partially denatured state of the protein, thus engaging the cellular quality control machinery to induce its proteasomal degradation. An aspect of the present invention relates to bifunctional small molecules that bind a number of proteins, including, for example, a self-labeling tag such as bacterial dehalogenase (HaloTag protein) and present a hydrophobic group on its surface. Hydrophobic tagging of the HaloTag protein with a hydrophobic moiety (e.g. an adamantyl moiety) was effected and the tagging induced the degradation of cytosolic, isoprenylated, and transmembrane fusion proteins in cell culture. The present invention also demonstrated the in vivo utility of hydrophobic tagging by degrading proteins expressed in zebrafish embryos and by inhibiting RasG12V-driven tumor progression in mice. Therefore, hydrophobic tagging of HaloTag fusion proteins affords small molecule control over any protein of interest, making it an ideal system for validating potential drug targets in disease models.
WO2014031875A1 Treatment of sickle cell disease and inflammatory conditions The invention provides methods and compositions for the treatment of sickle cell disease and other inflammatory conditions.
CN1799550A Highly efficient formulation of hepsera and preparation method thereof The invention discloses an adefovir dipivoxil preparation and preparing process, wherein the preparation comprises medicament, aliphatic acid, oily solution, assistant emulsifier and emulsifying agent by the weight ratio of 1:0.3-500:0-50:0-50:0-50. The preparation can be made into the dosage forms of soft capsules, hard capsules, oral liquids, granules and tablets.
US20050101783 N-(heterocycle-methyl)alkylamine derivative, process for producing the same, and bactericide A N-heterocyclicmethyl-alkylamine derivative according to the present invention is a N-heterocyclicmethyl-alkylamine derivative represented by the following general formula (I): or an acid addition salt thereof. [in the formula, R1 represents a heterocycle which has at least one nitrogen atom as a hetero atom and may have a substituent on a ring; R2 represents a hydrogen or the like; R3 represents an alkyl group having a carbon number of 1 to 5 or the like; R4 represents an alkyl group having a carbon number of 1 to 5 or the like; when R4 is an alkyl group having a carbon number of 1 to 5 or a halogenated alkyl group having a carbon number of 1 to 5, carbon atoms in R3 and R4 may be bonded to form a ring structure; m represents an integer of 1 to 3; R5 represents a cycloalkyl group or the like described by the following formula (III): (in the formula, Y and Z each represents a hydrogen atom or the like, the letter p represents an integer of 2 to 5, and the groups described by CYZ may be each the same or different), when m is 1 and R4 is a hydrogen atom, R5 is a cycloalkyl group described by the foregoing formula (III).]
CN101791290A Tetra-acetylated puerarin self-micro emulsifying medicament delivery system and preparation method thereof The invention relates to a tetra-acetylated puerarin self-micro emulsifying medicament delivery system and a preparation method thereof. The system is homogeneous transparent solution consists of tetra-acetylated puerarin, an oil phase, a surfactant and an auxiliary surfactant and forms spontaneously under the action of the peristalsis of the gastrointestinal tract. The preparation method comprises: weighing a proper amount of tetra-acetylated puerarin, adding a formula amount of oil phase, surfactant and auxiliary surfactant respectively, stirring the mixture under a 40 to 70 DEG C water bath condition to obtain tetra-acetylated puerarin self-micro emulsion and directly filling the tetra-acetylated puerarin self-micro emulsion in hard or soft capsules. The system and the method have the advantages of simple process and easy industrial production.
WO2009089851A1 Sulphoximine-substituted quinazoline derivatives as immunomodulators, their preparation and use as medicaments The present invention relates to sulphoximine-substituted quinazoline derivatives of the formula (I) processes for their preparation and their use as a medicament for the treatment of various diseases.
US20100029768 Compositions and Methods For Promoting Fat Loss This invention provides diets useful for promoting fat loss in animals having a total lysine to metabolizable energy ratio of from about 6 to about 10 g/Mcal. This invention also provides compositions for promoting fat loss in animals, methods for preparing the compositions, methods for using the diets and compositions, articles of manufacture comprising the diets and compositions, and means for communicating information or instructions about such diets, compositions, methods, and articles of manufacture.
CN102198142A Anti-tumour compounds with angeloyl groups Novel compounds such as compounds designated herein as Xanifolia-Y or -Y3, -Y1, -Y2, -Y8, -Y9 and -Y10 are disclosed. These compounds have anticancer activity. The compounds of the present invention are obtainable from plants in the sapindaceae family, such as Xanthoceras sorbifolia, or other natural sources or products. The compounds of the present invention may also be synthesized chemically.
EP1614422A2 Ibandronate for the promotion of osseointegration of endoprostheses The invention relates to use of ibandronic acid (1-hydroxy-3-(N-methyl-N-pentyl)aminopropyl-1,1-diphosphonic acid) or physiologically compatible salts or esters thereof for improving the osseointegration of cement-free anchored endoprostheses. Ibandronate or salts thereof is applied for a short time immediately after insertion of an endoprosthesis, with the surprising result that secondary stability of the implant is obtained in only 5 weeks or less after the operation.
WO2007039151A1 Blockers of transforming growth factor beta and its receptors for the treatment of infectious diseases The invention relates to the use of a transforming growth factor beta (TGFβ) blocker in the manufacture of medicaments for treating infectious CNS diseases and infections of ulcers of the skin. Moreover, the invention relates to a method of screening for a compound effective in the treatment of infectious CNS diseases and/or infections of ulcers of the skin. The method comprises contacting a candidate compound with a TGFβ or a TGFβ receptor and choosing candidate compounds which selectively reduce activity of TGFβ or the TGFβ receptor.
CN102038648B Powder injection for treating peptic ulcers and preparation method thereof The invention provides an injection for treating a peptic ulcers and a preparation method thereof. The powder injection provided by the invention comprises the active ingredients of Ilaprazole sodium and excipient, wherein the ratio of the both in parts by weight is (1:1)-(1:30), and the preferable ratio is (1:10)-(1:18). The preferable prescription of the powder injection provided by the invention comprises 1 part of Ilaprazole sodium, 1-30 parts of excipient, 0-10 parts of antioxidant and/or 0-0.3 part of metal ion complexing agent; and a right amount of inorganic base is added to regulate the pH value to 9.0-12.0. The Ilaprazole sodium freeze-dried powder injection provided by the invention has stable quality, and is suitable for treating peptic ulcer bleeding and stress ulcers and preventing upper gastrointestinal bleeding caused by serious diseases.
US7041684 4-[2-Hydroxy-3-([4-(5-carbamoyl-2-pyridyloxy)phenyl]-2-methylpropylamino)propoxy]carbazole and salts;treating obesity; antidiabetic agent for non-insulin dependent diabetes (Type II); The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective β3 receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and methods of treating Type II diabetes and obesity, comprising administering to a mammal in need thereof compounds of formula (I).
CN101774968A (E)-N-(5-chlorine-8-hydroxyl-2-styrene quinolyl) phenylsulfonyl aminated compound as well as preparation method and application thereof The invention relates to a (E)-N-(5-chlorine-8-hydroxyl-2-styrene quinolyl) phenylsulfonyl aminated compound shown as a formula (I) as well as a preparation method and application thereof. R1, R2 or R3 presents -H, -OH, -OCH3, -C1, -Br, -F or -NO2, and R1, R2 and R3 are same or different; R4 or R5 presents -H, -CH3, -C1, -F, -Br, -NO2 or -OCH3, and R4 and R5 are same or different. In the preparation method comprises the steps of: synthesizing 5-chlorine-8-hydroxyl-2-methylquinoline and benzaldehyde or substituted benzaldehyde into (E)-5-chlorine-8-hydroxyl-2-styryl quinoline; reacting the compound reacts with nitric acid to obtain an intermediate (E)-7-nitryl-5-chlorine-8-hydroxyl-2-styryl quinoline; reducing to obtain (E)-7-amido-5-chlorine-8-hydroxyl-2-styryl quinoline; reacting with benzene sulfonyl chloride to obtain the corresponding (E)-N-(5-chlorine-8-hydroxyl-2-styrene quinolyl) phenylsulfonyl aminated compound. The compound plays an inhibition effect on HIV-1integrase and can be used for preventing and treating infection caused by HIV.
CN102973489A Florfenicol solid dispersoid and preparation method thereof The invention relates to a florfenicol solid dispersoid and a preparation method thereof. The solid dispersoid comprises the components of: florfenicol and a carrier. The carrier combination is reasonable, a rapid supercritical gas expansion technology and a super micro powder technology are combined to be used, an organic solvent is not required, the solubility of a product in water is greatly improved, the bioavailability is effectively improved, and bacterial diseases (which are caused by sensitive bacteria) of beasts and birds can be effectively cured. Besides, the preparation process is simple and easy to operate, the product is harmless and environment-friendly, the curative effect is excellent, and the like.
CN101342170A Application of Xinjiang radix macrotomiae for treating flat wart, common wart and fig wart The invention discloses paste, emulsifiable paste and liquid medicine used for treating verrucous diseases including verruca plana, verruca vulgaris, condyloma acuminata, verruca plantaris, verruca filiformis, verruca digitalis and periungual wart, etc. Fat-soluble naphthoquinone alkannin, the effective component of radix macrotomiae, is adopted as the core of the invention. The fat-soluble naphthoquinone alkannin has an effect on anti-HPV. The main components of prescription by mass percent are as follows: 0.05 to 1.2 percent of the naphthoquinone alkannin, 0.2 to 0.8 percent of allantoin, 0.1 to 2 percent of Vitamin E, emulsifier and humectant, and the like, which constitute the paste, the emulsifiable paste and the liquid medicine. A test proves that the invention can treat the various verrucous diseases, including the verruca plana, the verruca vulgaris, the condyloma acuminata, the verruca plantaris, the verruca filiformis, the verruca digitalis and the periungual wart, and the like, and a curative effect is over 86 percent, so the invention is good medicine for treating the various verrucous diseases without any adverse reaction. The medicine with the high content of the naphthoquinone alkannin treats the condyloma acuminata best and has an effect on diminishing the inflammation of a hurt on an afflicted part, thus sterilizing the hurt and stimulating the healing of the hurt without leaving a scar.
CN103242417A Sterol derivative, and preparation method and application thereof The invention discloses a sterol derivative, and a preparation method and an application thereof. The sterol derivative comprises sterol compounds having a structural formula (I), or pharmaceutically acceptable salts of the sterol compounds, or extract products including the sterol compounds, or compositions including the sterol compounds. In the structural formula (I), R1 is -OH, =O, H, or a C1-C3 alkyl group; R2 is -OH, H, or a C1-C3 alkyl group; R3 is -OH, =O, H, or a C1-C3 alkyl group; R4 is -OH, H, or a C1-C3 alkyl group; and at least one of R1, R2, R3 and R4 is -OH. The compounds having the structural formula (I) can be used for preparing medicines having an HMG-CoA reductase activity inhibition effect, and the prepared medicines can effectively inhibit the activities of an HMG-CoA reductase.
CN101050200A 1 ¿C olefin substitutional N (2,6 dimethyl phenyl) - 2 ¿C piperidine formamide derivative This invention relates to compounds shown in general chemical formula I, their hydrates or solvates or pharmaceutically acceptable salts, which can be used to prepare local anesthetics. In general chemical formula I, m and n are 0-3.
WO2012041524A1 Hydrazonopyrazolones as protein tyrosine phosphatase inhibitors This invention relates to novel compounds useful in inhibiting protein tyrosine phosphatase activity, especially' Shp2 protein tyrosine phosphatase activity, pharmaceutical compositions comprising at least one of said compounds and their use for treating phosphatase-mediated diseases, especially Shp2- mediated diseases. These compounds act as protein tyrosine phosphatase (FTP) inhibitors, preferably as selective Shp2 inhibitors, and can therefore be used for the treatment of conditions, where protein tyrosine phosphatases are implicated, including cardiovascular, immunological, infectious, neurological, metabolic diseases, and cancer. Compounds of the invention are also useful as research tools for investigating the role of PTPs in signal transduction.
CN1852700A Triamcinolone acetonide and anecortave acetate formulations for injection Injectable compositions of triamcinolone acetonide or anecortave acetate are disclosed. The compositions are particularly suitable for injection into the posterior segment of the eye to treat ophthalmic diseases.
EP2042499A1 Salt of morpholine compound (2S)-[4-(Carboxymethyl)thiazol-2-ylthio]-N-{[4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}acetamide hydrobromide and a crystal thereof, which resist easy weight change caused by vapor sorption as compared to a free form, and are superior as drug substances of pharmaceutical products, and a production intermediate therefor are provided.
CN103142527A Entecavir potassium tablet and preparation method thereof The invention discloses an entecavir potassium tablet and a preparation method thereof. The ingredients of the entecavir potassium tablet comprise 0.1-0.5% of entecavir potassium, 92-95% of filler, 2-4% of disintegrating agent, 0.5-3% of adhesive and 0.5-3% of lubricant. The preparation method comprises the steps of: (a) respectively filtering the entecavir potassium, the filler, the disintegrating agent, the adhesive and the lubricant through a 80-mesh sieve for future use; (b) respectively extracting the main medicine and additives in step (a) according to a prescription dosage, and uniformly mixing the entecavir potassium, the filler, the disintegrating agent, the adhesive and the lubricant in an equivalent progressive increase method; (c) utilizing 70-80% ethanol as soft material, wet pelletizing and drying to obtain dry entecavir potassium granules; and (d) uniformly mixing the dry granules with magnesium stearate, and tabletting to obtain the entecavir potassium tablet. The entecavir potassium tablet prepared by the invention has good water solubility, the bioavailability of the medicine is high, and the entecavir potassium tablet supplements potassium ions at in vivo of hepatitis b patients, so that the clinic application value of the entecavir potassium tablet is improved.
EP1759703A4 Immunistimulative and interferonogenous agent The invention relates to medicine and biology, more specifically to novel biologically active substances. The aim of said invention is to develop novel immunostimulative and interferonogenous agents. The aim is attained by the use of the immunostimulative and interferonogenous agents in the form of 3,5-dimethyl-1-adamanthylommonia salts and water-soluble carboxyl-containing (co)polymers of general formula (I), wherein m and n are molar percentages, m=100-n and carboxyl-containing copolymers are selected from a polyvinylamine-cuccinic acid, vinyl alcohol and an N-vinylaminecuccinic acid copolymer and an N-vinylpyrrolidon and an N-vinylaminecuccinic acid copolymer group. The results of the comparative assays of the immunostimulative and interferonogenous activity and the toxicity of compositions are also disclosed. Said assays prove the sufficiently high activity of the inventive agents (greater than this of polyrem ) which are also favourably distinctive in terms of the antiviral sustained action thereof, whereby making it possible to use said polymer salts in the form of the immunostimulative and interferonogenous agents for smooth treatment and prevention of viral diseases. A general synthesis method and examples of synthesis for each inventive agent is also disclosed. The thus produced compounds are unambiguously identifiable by infrared spectroscopy, elemental analysis and potentiometric titration methods.
WO2014065427A1 Anagliptin-containing solid pharmaceutical preparation Provided is a solid pharmaceutical preparation which includes anagliptin or a salt thereof, and which exhibits excellent stability. The solid pharmaceutical preparation includes anagliptin or a salt thereof, and has a moisture content of not more than 3.4 mass%.
CA2789140A1 Synthesis of magnolol and its analogue compounds A method is described for producing magnolol, or a derivative or analogue thereof. The method includes obtaining MOM ether of 5,5'-diallylbiphenyl-2,2'-diol or a derivative or analogue thereof and subsequently converting the MOM ether of 5,5'-diallylbiphenyl-2,2'-diol into magnolol or a derivative or analogue thereof.
CN103601762A Ferrocene derivatives, preparation method and use thereof The invention discloses ferrocene derivatives as shown in a formula I in the specification and salts thereof, wherein Z is O or NH; R is selected from hydrogen, fluorine, chlorine, bromine, methyl, methoxyl and trifluoromethyl; n is an integer ranging from 0 to 5; R can be the same or different. The invention also provides compounds as shown in the formula I, and a preparation method and a medical use thereof; the compounds have anti-tumor activity, and can be used as a candidate medicament or a lead compound for treating diseases such as tumors and cancers.
US20080262032 Isoxazoline Derivative and Novel Process for Its Preparation The present invention relates to an isoxazoline derivative having the cyclic carboxylic acid hemiketal moiety of formula (1) for use as caspase inhibitor, a process for preparing it, and a pharmaceutical composition comprising it.
WO2009112522A1 (E)-N-(2-Amino-phenyl)-3-{1-[4-(1-methyl-1H-pyrazol-4-yl)-benzenesulfonyl]-1H-pyrrol-3-yl}-acrylamide salts A salt of (E)-N-{2-amino-phenyl)-3-{1 -[4-(1 -methyl-1 H-pyrazol-4-yl)- beπzenesulfonyl]-1 H-pyrrol-3-yl)-acrylamide selected from the group consisting of the hydrobromide, methansulfonate, hemi ethane-1,2-disulfonate, benzenesulfonate, toiuenesulfonate and 2-naphthalenesulfonate.
CN103110637A Paracetamol capsules and preparation method thereof The invention discloses paracetamol capsules and a preparation method of the paracetamol capsules. The paracetamol capsules comprise pharmaceutical effective components and formulation excipients, wherein the pharmaceutical effective components consist of acetaminophen and caffeine in a weight ratio of 1: 0.13; and the formulation excipients comprise a filler, a disintegrant, a surfactant, a diluent, a lubricant, a glidant, and a flavoring agent. The paracetamol capsules disclosed by the invention have the advantages of quickness in dissolution, fastness in absorption, high bioavailability, good stability and convenience in taking.
EP2437719A1 Treatment of eye discomfort by topical administration of a cooling agent to the external surface of the eyelid The present invention pertains generally to the field of ocular treatment, and more specifically to the use of a liquid cooling agent composition comprising a cooling agent for the treatment of (e.g., the alleviation of symptoms of; the amelioration of) eye discomfort. The preferred cooling agent is (1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarboxylic acid 2,3-dihydroxy-propyl ester (referred to herein as formula (CPS-030)). The liquid cooling agent composition is topically administered to at least a portion of the external surface of the eyelid (preferably the closed eyelid) of the eye to be treated. Preferably, the liquid cooling agent composition is carried on or in a wipe, pad, or towelette, for example, an eye wipe.
CN103251614A Application of Aspeverin in preparation of medicines for inhibiting liver fibroblast proliferation The invention discloses an application of Aspeverin in preparation of medicines for inhibiting liver fibroblast proliferation. Pharmacological testing proves that the Aspeverin can obviously inhibit liver fibrosis from being caused and developed, and can be used for preparing the medicines for resisting liver fibrosis and treating liver cirrhosis. The application of Aspeverin in preparation of medicines for inhibiting liver fibroblast proliferation is disclosed for the first time, a framework type belongs to a brand-new framework type, the Aspeverin has an unexpected strong effect of inhibiting the liver fibroblast proliferation activity, and the revelation possibility of other compounds cannot be generated, so that the application has obvious substantive features; and moreover, the application has an obvious improved effect of inhibiting the liver fibroblast proliferation.
CA2572075A1 Hetero isonipecotic modulators of vanilloid vr1 receptor This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals.
US20110077246 Bicyclic heterocyclic compounds pharmaceutical compositions containing these compounds, their use and process for preparing the same The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula wherein said substituents are as defined herein.
WO2006059164A2 Pyrrolopyridine-2-carboxylic acid amides Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.
CA2278509C Production method of optically active imidazole compound, synthetic intermediate therefor and production method thereof The present invention provides a method for producing an optically active 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid or a pharmaceutically acceptable salt thereof, which includes subjecting a compound of the formula (I) (see formula I) wherein each symbol in the formula is as defined in the specification, to optical resolution by fractional crystallization to give an optically active compound thereof and subjecting the compound to hydrolysis reaction. According to this method, a resolution method useful for industrial large-scale production of the optically active compound of 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid, which is useful as a thromboxane synthetase inhibitor and an agent for the prophylaxis and treatment of diabetic complications, can be obtained.
WO2009116888A1 Pharmaceutical composition for preventing and treating bone resorption of different etiology The invention relates to medicine and pharmacology and discloses a pharmaceutical composition for treating bone resorption of different etiology, which composition contains liposomes with bisphosphonates in a gel dosage form as a biologically active ingredient suitable for transdermal delivery of bisphosphonates and for effective topical treatment. Methods using the inventive composition for preventing and treating osteoporosis, Paget's disease and pathological fractures caused by oncological diseases and some other pathological processes related to bone resorption and reparation are also disclosed.
WO2009120390A3 Cyclopropanated carbohydrates Disclosed are cyclopropanated carbohydrate compounds of formulas (I) and (II). Also disclosed are methods of treating or preventing a central nervous system ailment by administering to an organism in need thereof an effective amount of a cyclopropanated carbohydrate compound of formula (I) or (II) and pharmaceutical compositions containing a cyclopropanated carbohydrate compound of formula (I) or (II).
CA2801143A1 Disinfecting agent comprising eugenol, terpineol and thymol The present invention relates to a method of disinfecting a surface and to antimicrobial composition, particularly for personal cleaning, oral care, or hard surface cleaning. It is an object of the present invention to provide for an antimicrobial composition that has relatively fast antimicrobial action. The inventors have found that use of small amounts of eugenol in combination with thymol and terpineol enables this fast kinetics at much lower amount of thymol and terpineol than without eugenol.
WO2005075454A3 SALT FORMS OF 4-(4-METHYLPIPERAZIN-1-YLMETHYL)-n-[4-METHYL-3-(4-PYRIDIN-3-YL)PYRIMIDIN-2-YLAMINO)PHENYL]-BENZAMIDE The present invention relates to acid addition salts of 4-[4-methyl-1-piperazinylmethyl]-N-[4-methyl-3-[[4-¢3-pyridinyl-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(-) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate sat, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.
US20090137576 Novel Piperidine Derivative Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.
EP2749556A1 An improved process for the preparation of pure cyamemazine and salts thereof The present invention provides an improved process for the preparation of cyamemazine of formula-1 or its pharmaceutically acceptable salt thereof, which is substantially free of impurities.
US20080261927 Nutrient phytosterol or phytostanol ester with dispersion aid selected from triglyceride, an essential oil extract, night primrose oil, and/or fish oil; beverages, cosmetics An aqueous suspension of a hydrophobic nutrient is disclosed. In particular, the nutrient, in ester form, is combined with a selected dispersion aid and a dispersion agent(s), and then dispersed in an aqueous medium to form the suspension.
WO2014078331A1 N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
WO2008107677A3 Thiadiazole and oxadiazole derivatives for the treatment of neurodegenerative disorders A compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein X is an oxygen or sulphur atom A is CH(R6)-, -O- or NR7 or when A is NR7, then R1 and NR7 can together form a ring such that R1 and R7 are (CH2)n, where n is 2-4, preferably 2-3; Y is a bond, CH(R6)-, -O- or NR7 or A and Y together form a single bond between the aromatic group and the carbonyl group but when A is-O- then Y is not -O-; R1 and R2 are independently hydrogen, halogen, OR8, NR9R10, NR9COR11, NR9SO2R11 or C1-6 alkyl optionally substituted by fluorine, hydroxyl, C1-6 alkoxy or NR9R10; R3 is C1-6 alkyl, C3-8 cycloalkyl C4-10 alkylcycloalkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R4 is hydrogen, halogen, CF3, OR9, NR9R10, NR9COR11, NR9SO2R11 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R5 is hydrogen, halogen, CF3, OR8, COOR9, CONR9R10 or SO2R11; The compounds find use in the treatment of amyloid related diseases, such as Alzheimer disease.
CN103462969A Application of Incarviatone A in medicaments for treating breast cancer The invention discloses an application of Incarviatone A in preparation of medicaments for treating breast cancer, and belongs to the technical field of a new application of medicaments. In-vitro methyl thiazolyl tetrazolium (MTT) anti-tumor activity evaluation discovers that the Incarviatone A has a prominent inhibiting effect on growth of human breast cancer cell strains 4T1, MCF-7, MDA-MB-231 and MCF-7B. Therefore, the Incarviatone A can be used for preparing anti-breast cancer medicaments, and has a good development and application prospect. The application of the Incarviatone A in preparation of the medicaments for treating the breast cancer is made public for the first time, the skeleton type is completely novel, and the Incarviatone A has an unexpectedly strong breast cancer cell inhibiting activity.
WO2012052180A1 Combinations comprising dhodh inhibitors and cox inhibitors Combinations comprising (a) DHODH inhibitors and (b) COX inhibitors and their treating skin diseases or disorders are disclosed.
US20080075749 Methods and Compositions for Tissue Augmentation Methods and compositions for use in tissue volume replacement are provided. The present invention comprises compositions comprising a combination of materials, comprising preferably a solid polymer particle phase and a gel phase, and also comprises single phase compositions. More particularly, preferred embodiments comprise a solid polymer particle phase made of materials comprising Gore-Tex (micronized e-PTFE), PDS II (polydioxanone, a monofilament), NUROLON (a long chain aliphatic polymer Nylon 6 or Nylon 6,6) ETHILON (a long chain aliphatic polymer Nylon 6 and Nylon 6,6), PROLENE (Polypropylene, isotactic crystalline stereoisomer of polypropylene, a synthetic linear polyolefin.), VICRYL (copolymer made from 90% glycolide and 10% L-lactide), silk, MONACRYL (poly ε-caprolactone.), polylactide, polyglycolide, poly lactide-co-glycolide, and BIOPOL (polyhydroxyvalerate), MEDPOR (biocompatible (micronized) polyethylene), BIOGLASS (bioactive glass particulate), NOVABONE and NOVABONE-CM, and the gel phase comprises polyvinylpyrrolidone (PVP). Preferred single phase compositions comprise PVP. Methods of the present invention comprising injection of such compositions for tissue augmentation.
US20070043005 Treatment of hyperproliferative diseases using high doses of active vitamin d The present invention provides a method of inhibiting the hyperproliferative cellular activity of neoplasms and other hyperproliferative diseases with an active vitamin D compound utilizing a high dose, episodic treatment protocol.
WO2009046098A1 Novel cyclic boronate inhibitors of hcv replication Compounds of formula (I) or a salt thereof are provided; wherein R1, R2, R3, R4, R6, R8, R20, R30, Y, Z and n are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicaments for treating viral infection, especially HCV infection are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
CN1757637B Method for purifying VE nicotinate raw material The present invention discloses a purification method and preparation of raw material of VE ester of nicotinic acid. It improves the product from original light yellow to white or similar white, greatly improves the safety with the medicine. The purification method is to dissolve the VE ester of nicotinic acid in appropriate volume of organic solvent, adding some absorbent (or without adsorbent), stirring at room temperature to 80 DEG C for 5 - 500 minutes, filtrating to remove the adsorbent, staying at 5--50 DEG C for 1-100 hours, collecting the deposit, after drying the product is purified. Check the purity of the raw material of VE ester of nicotinic acid with HPLC, its purity is higher than 99%. The raw material purified maybe used further for various preparation, including emulsion (medium length chain oil, long length chain oil, or mixed oil ejection, oral emulsion), liposomes (including liposomes nanoparticle), hard, soft capsule (including self-emulsion), tablet, granular preparation, mixed suspension preparation.
US20100330009 Coumestan-like antioxidants and uv absorbants The present invention relates to derivatives of the 1H-pyrano[4,3-b]benzofuran-1-one structure and their nitrogen analogues which possess powerful antioxidant properties combined with a highly effective UV absorbing functionality in one molecule. These compounds are especially useful in cosmetical and dermatological formulations.
US20130039882 Method to mitigate injury from radiation exposure Mitigating radiation induced injury to a mammal that has been exposed to radiation by administering a pharmaceutically effective amount of a composition comprising at least one CXCR4 antagonist to the mammal.
US20060121125 Formulation which can be administered gastrointestinally, containing green tea extract and an no donor A formulation which can be administered gastrointestinally and comprises green tea extract and at least one NO donor which is a substrate of NO synthetase, and/or a precursor thereof is described. The formulation is administered before surgical procedures, in order to avert or reduce the risk of postoperative complications.
US20100316609 Conditionally Replicating Viruses for Cancer Therapy Described herein are viral vectors comprising a nucleic acid encoding a viral DNA polymerase wherein the encoded viral DNA polymerase comprises at least one amino acid modification. Also provided are methods of making and using the viral vectors.
US20110301095 Methods and compositions for assessing and treating metastasis, metastatic cancer, and potential for metastasis Disclosed are methods, compounds, and compositions for detection, diagnosis, prognosis, monitoring, treatment, monitoring treatment, and selecting treatment of cancer and metastasis, and for identifying compounds and compositions for such uses. For example, disclosed are methods, compounds, and compositions for detecting a risk of metastasis of cancer in a subject, treating a subject at risk of metastasis of cancer, identifying an inhibitor of HIF1α:FoxA2 function or complex formation, detecting a risk of neuroendocrine differentiation (NED)-associated cancer, determining a prognosis of a cancer, determining a treatment for a cancer, monitoring or determining the effect of treatment of a NED-associated cancer, treating NED-associated cancer, identifying an inhibitor of HIF1α:FoxA2 complex formation, detecting neuroendocrine differentiation (NED)-associated cancer, monitoring the risk of metastasis of cancer in a subject, and treating NED-associated cancer.
US20050175643 Fermentation microbe and metabolites, thickener, water, and carbon dioxide; adding water and thickener to carbon dioxide-impermeable sealable container; low speed depressurization to degas raw materials; filling with carbon dioxide; skin and atopic disorders; wound healing agents; dermatitis, pruritus Carbon dioxide is dissolved in a non-bubble state in a viscous material comprising at least water and a thickener. A production method of this carbon dioxide composition for external use comprises the steps of introducing at least water and a thickener as raw materials into a carbon dioxide-impermeable sealable container, reducing the pressure inside the container to degas the raw materials, and filling carbon dioxide into the container and maintaining a sealed state, and the step of mixing the raw materials to prepare a viscous material, wherein at least during the step of filling carbon dioxide into the container. Another carbon dioxide composition for external use comprises at least a fermentation microbe, a metabolite of the fermentation microbe, a thickener, water, and carbon dioxide. With these carbon dioxide compositions for external use, strong cosmetic and medical effects are readily obtained with a small amount of the composition.
CN101507762B Veterinary medicine for treating colibacillosis and white dysentery The invention relates to a veterinary medicament, in particular to a medicament which consists of natural plants and natural mineral compositions, and particularly relates to a veterinary medicament for preventing and treating colibacillosis and/or white diarrhea, in particular to a medicament for treating the colibacillosis and/or the white diarrhea of poultry. The medicament consists of the following compositions: honeysuckle, gypsum, radix paeoniae rubra, Chinese pulsatilla, weeping forsythia, cyrtomium rhizome, kuh-seng, Chinese ephedra, Astragalus membranaceus, isatis root, and liquorice.
WO2008012690A3 Use of 1,2,3-substituted indolizine derivatives, inhibitors of fgfs, for the preparation of a medicament intended for the treatment of degenerative joint diseases The present invention concerns the use of 1,2,3-substituted indolizine derivatives of formula (I), as defined in the description; (I) and in particular the 2-amino-5-[(1-methoxy-2-methylindolizin-3-yl)carbonyl]benzoic acid, and their pharmaceutically acceptable salts and solvates for the preparation of a medicament intended for the treatment of degenerative joint diseases, such as osteoarthritis, spondyloses, cartilage loss following joint trauma or a relatively long period of joint immobilization following meniscus or patella injuries or ligament ruptures, and chronic diseases of the locomotory apparatus such as inflammatory, immunological or metabolism-associated acute and chronic arthritides, arthropathies, myalgias and disturbances of bone metabolism.
WO2011033306A1 Inhibition of tendon adhesions The invention provides composition having an osmolality of at least 1200m Osmol for use as a medicament for the inhibition of tendon adhesion formation. The compositions of the invention may comprises a sugar phosphate, such as mannose-6-phosphate (M6P) and/or glucose-6-phosphate (G6P). Composition comprising M6P are particularly favoured. The compositions may improve tendon repair by increasing the quality of replacement tendon formed after injury, and may be well suited to administration by injection.
CN1861096A Application of diarsenic trioxide in ion-exchange protein An application of As2O3 as excitomotor in improving the function of anionic exchange protein 2 is disclosed. Said anionic exchange protein 2 can regulate the pH value, volume and stability of cell.
CN201906228U Composite structure of medicine for treating type II diabetes The utility model provides a composite structure of a medicine for treating type II diabetes, which is characterized by comprising an osmotic pump tablet core of metformin hydrochloride and an outer glimepiride layer, wherein the osmotic pump tablet core of metformin hydrochloride comprises a white pill and a semipermeable membrane layer at the outer layer of the white pill; the white pill is prepared from the metformin hydrochloride and pharmaceutically acceptable auxiliary materials; an isolating layer is arranged between the white pill and the semipermeable membrane layer; another isolating layer is arranged at the exterior of the semipermeable membrane layer; and a dampproof layer is coated at the exterior of the glimepiride layer. The composite structure combines the characteristics of both an osmotic pump tablet and glimepiride, and achieves the purpose of combination therapy in the form of a composition.
WO2013092556A1 Metal-chelating compounds having at least one polyamino chain The invention relates to metal-chelating compounds comprising one or more 8-hydroxyquinoline units substituted in position 2 with a nitrogenous group comprising a polyamino chain, wherein the polyamino chain is N-substituted on said nitrogenous group, to the composition containing same, and to the uses thereof in the therapeutic field and in particular in the treatment of diseases associated with an abnormality in the regulation of metal metabolism resulting in a metal overload in human or animal cells.
US20090246146 Halides in the treatment of pathogenic infection The present invention relates to the use of halides and halide salts for the treatment of microbial infections, including those caused by bacteria, fungi and viruses. The present invention takes advantage of endogenous immune function and augments this system using a non-toxic and inexpensive reagent that can be delivered to mucosal surfaces, for example, orally, topically, opthalmically and via inhalation.
US20090162390 Molecular Scaffolds for HIV-1 Immunogens Methods and compositions are provided which employ chimeric polypeptides having at least one heterologous epitope for a human immunodeficiency virus type 1 (HIV-1) neutralizing antibody. These chimeric polypeptides behave as molecular scaffolds which are capable of presenting the various heterologous HIV-1 epitopes. The invention demonstrates that a heterologous epitope recognized by the HIV-1 neutralizing antibody can be more fully exposed to neutralizing antibodies when presented within the backbone of the chimeric polypeptide than when the epitope is presented within the context of an HIV-1 backbone. Polynucleotides encoding these chimeric polypeptides are also provided. Immunogenic compositions are provided which comprise a chimeric polypeptide having at least one heterologous epitope that interacts with an HIV-1 neutralizing antibody. Immuno genie compositions comprising chimeric polynucleotides encoding the chimeric polypeptides of the invention are also provided. Vaccines comprising such immunogenic compositions are also provided. Further provided are methods which employ the immunogenic compositions of the invention. Such methods include, for example, methods for eliciting an immune response in a subject, methods for generating antibodies specific for the chimeric polypeptide or the chimeric polypeptide, and methods for inhibiting or preventing infection by HIV-1 in a subject.
US6989362 Methods of treating dopamine dysregulation using agents that regulate phosphorylation/dephosphorylation in dopamine signaling The present invention discloses that DARPP-32 is substrate for the cyclin dependent kinase Cdk5. The phosphorylation takes place at a specific threonine residue of DARPP-32 (Threonine 75). The Cdk5 catalyzed phosphorylation of DARPP-32 converts this protein into an inhibitor of the cAMP dependent protein kinase (PKA) and furthermore prevents it from being converted to an inhibitor of protein phosphatase 1 (PP1). Methods of identifying agents that modulate the phosphorylation of DARPP-32 by Cdk5 are disclosed. Methods of treating dopamine dysfunction in animal subjects are also provided.
WO2011108963A8 Urethanes, ureas, amidines and related inhibitors of factor xa The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.
EP1514550A2 Combinations for diabetes which contain a sulfonylurea, a glitazone and a biguanide Combinations of a glitazone antidiabetic agent, a biguanide antidiabetic agent, and a sulfonylurea antidiabetic agent, are useful for treating diabetes mellitus and improving glycemic control.
US7964592 2,4-di (phenylamino) pyrimidines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders Novel pyrimidine derivatives of formula I to process for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
US6921760 Psychotherapeutic agents. The present invention relates to compounds of the formula Orosco wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.
US20080131499 Method and composition for solubilising a biologically active compound with low water solubilty Compositions for forming molecular associates with lipophilic compounds and an improved method of loading lipophilic biologically active compounds into previously formed, aqueous suspensions of lipid particles. A preferred embodiment for injection purposes comprise lipid particles having sizes below 1000 nm in diameter, in a vial or other suitable container are described. The method involves mixing a lipophilic compound either in solution or as an amorphous, preferably lyophilised powder in a first container with an aqueous suspension of lipid particles contained in a second container to form molecular associates. Only minimum agitation is required. The entire procedure may be carried out instantly in situ, in sealed sterile units just prior to use in the hospital ward or by the bedside.
CN1899298A Acne eliminating liquid The present invention belongs to the field of externally applied medicine, and is especially one kind of acne eliminating medicine liquid. The acne eliminating medicine liquid of the present invention has high acne eliminating effect, high safety, low cost and other advantages.
CN102370983A Anti-tumor medicine composition and purpose thereof The invention discloses a solid tumor resisting medicine composition with arctigenin and nitrosourea alkylating agent anti-tumor medicines as active components. The weight ratio of arctigenin to nitrosourea alkylating agent anti-tumor medicines is 1:0.001-1000, and preferably 1:0.01-600. The anti-tumor medicine composition provided by the invention is advantaged in clear components, wide anti-tumor spectrum, substantial treatment effect against various tumors, low price, low side-effects, and good clinical application prospect.
CA2800187A1 Preparation apparatus and preparation method for dialysis fluid of variable bicarbonate ion concentration type, dialysate of variable bicarbonate ion concentration type, and dialysis system of variable bicarbonate ion concentration type An object of the present invention is to provide a technology for preparing a dialysis fluid that is capable of flexibly changing the bicarbonate ion concentration and maintaining the concentrations of electrolytes such as potassium, calcium, and magnesium at constant levels even during dialysis according to the disease state of a patient. In connection with a three-component dialysate containing an agent S containing sodium chloride, an agent B containing sodium bicarbonate, and an agent A containing electrolyte components other than sodium chloride and sodium bicarbonate, suitably adjusting the amount of the agent B during dialysis fluid preparation makes it possible to maintain the concentrations of trace metal ions such as potassium ions, calcium ions, and magnesium ions in a dialysis fluid at constant levels and flexibly change the bicarbonate ion concentration therein. Moreover, in the three-component dialysate, adjusting the ratio between the amount of the agent S and the amount of the agent B when the dialysate is used also makes it possible to maintain the sodium ion concentration at a constant level or flexibly change the sodium ion concentration.
EP1695964A1 Quinoline derivatives for use as intermediates in the synthesis of heterocyclylalcoyl piperidines 1,4-Disubstituted 4-(quinolin-4-yl-alkyl)-piperidine derivatives (I) are new. Piperidine derivatives of formula (I), their enantiomers, diastereomers and mixtures, syn- or anti-isomers and salts, are new. [Image] X1 - X5CR or N, provided that only one may be N; R, R1H, halo, alkyl, cycloalkyl, Ph, SPh, Het, -S-Het, OH, alkoxy, OCF3, alkylthio, SCF3, cycloalkoxy, cycloalkylthio, CN, COOH, alkoxycarbonyl, cycloalkoxycarbonyl, NRaRb, CONRaRb, CH2T, OPh, heterocyclyloxy, benzyloxy or heterocyclylmethoxy; or R1 may also be 1-6C perfluoroalkyl, 1-6C perfluoroalkoxy or 1-6C perfluoroalkylthio; or R in the X5 position may also be COCF3; Het : mono- or bicyclic aromatic heterocyclyl; Ra, RbH, alkyl, cycloalkyl, phenyl or Het; or NRaRb5- or 6-membered heterocyclyl, optionally containing another O, S, SO, SO2 or NQ heteroatom; Q : H, Ph or Het; T : F, OH, alkoxy, alkylthio, cycloalkoxy, cycloalkylthio, Het, COOH, alkoxycarbonyl, cycloalkoxycarbonyl, NRaRb or CONRaRb; R2COOH, alkoxycarbonyl, cycloalkoxycarbonyl, CN, COOH, SO3H, CONR'aR'b, CH2OH, -U-V, CF2Rc, CMe2-Rc, CORc, CH(OH)Rc, -C(cycloalkyl)-Rc or -CH=CH-Rc; R'a, R'bas Ra, Rb, except that one of R'a, R'b may also be OH, alkoxy or cycloalkoxy; or NR'aR'bheterocycle as defined for NRaRb; U : 1-2C alkylene; V : COOH, alkoxycarbonyl, cycloalkoxycarbonyl, CN, SO3H or CONR'aR'b; RcCOOH, alkoxycarbonyl, cycloalkoxycarbonyl or CONR'aR'b; R3Ph, Het or alkyl (optionally substituted by R'3); R'3halo, OH, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, mono- or dialkylamino, cycloalkyl, cycloalkoxy, cycloalkylthio, cycloalkylsulfinyl, cycloalkylsulfonyl, mono- or dicycloalkylamino, N-alkyl-N-cycloalkylamino, acyl, cycloalkylcarbonyl, Ph, OPh, SPh, SOPh, SO2Ph, NHPh, NPh2, N-alkyl-N-phenylamino, N-cycloalkyl-N-phenylamino, phenylalkoxy, phenylalkylthio, phenylalkylsulfinyl, phenylalkylsulfonyl, phenylalkylamino, N-alkyl-N-phenylalkylamino, N-cycloalkyl-N-phenylalkylamino, benzoyl, -O-Het, -S-Het, -SO-Het, -SO2-Het, -NH-Het, N-alkyl-N-(Het)-amino, N-cycloalkyl-N-(Het)-amino, -CO-Het, Het-alkoxy, Het-alkylthio, Het-alkylsulfinyl, Het-alkylsulfonyl, Het-alkylamino, N-alkyl-N-(Het-alkyl)-amino, N-cycloalkyl-N-(Het-alkyl)-amino, COOH, alkoxycarbonyl, NR'aR'b, CONR'aR'b, -C(R''b)=C(R'c)-R''a, -CC-Rd, -CF2-phenyl or -CF2-Het; R''aPh, phenylalkyl, Het, Het-alkyl, phenoxyalkyl, phenylthioalkyl, phenylsulfinylalkyl, phenylsulfonylalkyl, phenylaminoalkyl, N-alkyl-N-phenylaminoalkyl, Het-O-alkyl, Het-S-alkyl, Het-SO-alkyl, Het-SO2-alkyl, Het-NH-alkyl, N-alkyl-N-(Het)-amino, -S-Het, -SO-Het, -SO2-Het, SPh, SOPh or SO2Ph; R''b, R'cH, alkyl or cycloalkyl; Rdalkyl, Ph, phenylalkyl, phenoxyalkyl, phenylthioalkyl, N-alkyl-N-phenylaminoalkyl, Het, Het-alkyl, Het-O-alkyl, Het-S-alkyl, Het-NH-alkyl or N-alkyl-N-(Het)-aminoalkyl; Y : -CH(Re)-, CF2, CO C(=NOH), alkoxyiminomethylene, cycloalkoxyiminomethylene or 3-6C cycloalkylidene; ReH, F, OH, alkoxy, cycloalkoxy, COOH, alkoxycarbonyl, cycloalkoxycarbonyl, NQaQb or CONQaQb; Qa, Qbas R'a, R'b; or one is H and the other is alkoxycarbonyl, acyl, cycloalkoxycarbonyl, -CO-Ph or -CO-Het; and n : 0-4; phenyl and heterocyclyl moieties are optionally substituted by 1-4 of halo, OH, alkyl, alkoxy, alkoxyalkyl, haloalkyl, CF3, OCF3 SCF3, COOH, alkoxycarbony, CN, alkylamino, NR'aR'b, Ph, hydroxyalkyl, alkylthioalkyl, alkylsulfonylalkyl or alkylsulfonylalkyl; alkyl or acyl moieties have 1-10C (unless specified otherwise); cycloalkyl moieties have 3-6C. An independent claim is included for the preparation of (I). - ACTIVITY : Antibacterial. (I) show activity in vitro against methicillin-resistant Staphylococcus aureus AS5155 at 0.03-4 Microg/ml, Streptococcus pneumoniae 6254-01 at 0.03-8 Microg/ml and Moraxella catarrhalis IPA 152 at 0.12-64 Microg/ml, and in vivo against Staphylococcus aureus IP8203 infections in mice at 18-150 mg/ml s.c. (DC50). No specific results for individual compounds are given in the source material. - MECHANISM OF ACTION : None given.
CN101015576A Medicine for preventing and treating cardiovascular and cerebrovascular diseases by increasing hypoxia-resistant ability and its preparing method The invention discloses a preparation for improving tolerance to anoxia and preventing and treating cardio-cerebrovascular disease and its preparation method. The preparation is prepared from (by weight part) ginkgo leaf 600-900, american ginseng 40, taurine 5-15, tea polyphenol 5-15, ferrous gluconate 2-6, and folic acid 0.01-0.05 by dectocting ginkgo leaf and american ginseng, filtrating, concentrating, drying, pulverizing taurine, tea polyphenol, ferrous gluconate, and folic acid respectively, mixing, and drying. Compared with present unilateralism or compound preparation, the inventive preparation has remarkable effects in improving cellulate tolerance to anoxia, preventing and treating cardio-cerebrovascular disease, reducing blood pressure and lipid with rapid action, high bioavailability, no subsidiary reaction; and it can be used for long term administration.
EP2445483A2 Topical compositions and methods for wound care The present disclosure relates to compositions for and methods of repairing the stratum corneum, compositions and methods for inhibiting excessive transepidermal water loss, compositions for and methods of treating skin that is distressed or wounded as a result of a disease or other biological condition or process (as distinguished from wounds resulting from trauma), compositions for and methods of treating chronic wounds, and compositions for the inhibition and treatment of necrosis and extended quiescence that result in cellular necrosis instead of normal proliferation.
US20130040977 Pro-Neurogenic Compounds This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
CN102727502A Anti-influenza virus composition, and food, drink, feed and pharmaceuticals thereof The invention provides an anti-influenza virus composition, and food, drink, feed and pharmaceuticals thereof, being able to easily obtain and be absorbed in daily life with high safety. The anti-influenza virus composition is formed by active constituents, Fructo-oligosaccharide (Beta-D-galactosyl-(1, 4)-Alpha-D-glucosyl-(1, 2)-Beta-D-fructoside) and a carrier, being able to prevent influenza virus infection and/or relieve symptoms. The prevention effect is obtained by preabsorbing the anti-influenza virus composition in daily life. Therefore, the anti-influenza virus composition, and food, drink, feed and pharmaceuticals thereof have the advantage of no limitation for types of influenza.
EP1885350A2 Formulations and methods for treating amyloidosis Methods, formulations, and compositions for the treatment of amyloidosis are described, whereby a therapeutically effective amount of a compound having the formula (I) wherein Y is SO3X or OSO3X independently chosen for each occurrence; X is cationic group independently chosen for each occurrence; n is 1, 2, 3 or 4; and m is 1 or 2, is applied.
US20080226664 Colon cancer antigen panel The invention provides methods, compositions and kits for inducing and/or enhancing an immune response in a subject. The invention in some aspects includes polypeptide and nucleic acid molecules that induce and/or enhance an immune response. In some aspects of the invention, the polypeptide and/or nucleic acid molecules of the invention are useful to induce and/or enhance an immune response in a subject who has or is suspected of having cancer.
US20110190388 Ursolic acid derivative and pharmaceutical composition thereof Several ursolic acid derivatives and pharmaceutical compositions thereof are provided. The ursolic acid derivatives and the pharmaceutical compositions thereof have at least one of an anticancer and an anti-inflammatory effects. A method for increasing a reactive oxygen species in a cell is also provided. The method comprises a step of providing the cell with a pharmaceutical composition including an ursolic acid derivative.
US20120094967 Compositions and methods for treating asthma and other lung diseases The present invention provides methods for dilating the bronchi or bronchioles and relaxing a pulmonary smooth muscle in a subject by treating the subject with a pharmaceutical composition, which includes a Histone deacetylase (HDAC) inhibitor. The ability to dilate the bronchi or bronchioles and relax a pulmonary smooth muscle according to the methods of the invention allows treating, alleviating, or inhibiting bronchoconstrictive diseases or disorders and symptoms associated or derived from bronchoconstrictive diseases.
WO2007091557A1 Pharmaceutical composition for treatment or prevention of liver cancer The object is to provide an excellent therapeutic or prophylactic agent for liver cancer. Disclosed is a pharmaceutical composition for treatment or prevention of liver cancer, which comprises menatetrenone (which is one type of vitamin K) and a phospholipids. The phospholipids is preferably egg yolk lecithin or soybean lecithin.
CN103585268A Acne-treating composition and preparation method thereof, and acne-treating skin-care product The invention relates to the field of medical cosmetology, specifically to an acne-treating composition and a preparation method thereof and an acne-treating skin-care product. The acne-treating composition is prepared from the following raw materials by weight: 15 to 25 parts of borneol, 25 to 35 parts of a paste extract of honeysuckle flower, 26 to 40 parts of a paste extract of peppermint and 0.8 to 1 part of trichlorfon. The preparation method comprises the following steps: respectively crushing borneol and trichlorfon so as to obtain borneol powder and trichlorfon powder; and uniformly mixing the borneol powder, the trichlorfon powder, the paste extract of honeysuckle flower and the paste extract of peppermint in proportion so as to obtain the acne-treating composition. Compared with traditional acne-treating medicines, the invention has the following advantages: the acne-treating composition and the acne-treating skin-care product have little side effect on the skin and remove whelks without leaving pockmarks, and bother brought to patients by pockmarks is overcome.
US20100233264 TEMPERATURE AND pH-SENSITIVE BLOCK COPOLYMER HAVING EXCELLENT SAFTY IN VIVO AND HYDROGEL AND DRUG DELIVERY SYSTEM USING THEREOF Disclosed herein are pH- and temperature-sensitive block copolymer with excellent safety and a method for preparing the same and a hydrogel and a drug carrier using the block copolymer. According to the present invention, the pH- and temperature-sensitive block copolymer comprises: obtained by copolymerization of: (a) polyethylene glycol-based compound (A); and (b) poly (β-amino ester)-based oligomer (B) or poly (amido amine)-based oligomer (C) or coupling of mixture (D) thereof. In order to control biodegradation rate, the block copolymer is mixed with poly (amido amine)-based oligomer instead of the poly (β-amino ester)-based oligomer and then coupling them.
US6984654 Cancer treatments and pharmaceutical compositions therefor A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide is disclosed. The particular fungicide used is a benzimidazole derivative having the formula: wherein R is selected from the group consisting of H, carboxyl (—CO2H), hydroxyl, amino or esters (—CO2R′) wherein R′ is selected from the group consisting of alkoxy, haloalkyl, alkenyl, and cycloalkyl wherein the alkyl groups have from 1–8 carbons or CH3CH2(OCH2CH2)n— or CH3CH2CH2(OCH2CH2CH2)n— or (CH3)2CH—(OCH(CH3)CH2)n— wherein n is from 1–3, the pharmaceutically acceptable salts thereof, or mixtures thereof.
WO2007067981A2 RNA INTERFERENCE MEDIATED INHIBITION OF VASCULAR ENDOTHELIAL GROWTH FACTOR AND VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) This invention relates to compounds, compositions, and methods useful for modulating VEGF and/or VEGFR gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of VEGF and/or VEGFR gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of VEGF and/or VEGFR genes. The application also relates to methods of treating diseases and conditions associated with VEGF and/or VEGFR gene expression, such as ocular diseases and conditions, including age related macular degeneration (AMD) and diabetic retinopathy, as well as providing dosing regimens and treatment protocols.
CN101397298A Acidamide substituted pyrrole[2,3-b] pyridines compounds, preparation method and use thereof The invention relates to an amide-substituted pyrrole (2, 3-b) pyridine compound, a preparation method and the application thereof. The structural formula of the compound of the invention is shown in the formula (I) and the compound is a depressor secreted by MTP and/or B (Apo B) and is suitable for weight management and treatment for obesity and relevant diseases. The invention also relates to the medicine combination containing the compounds, the application of the compounds, the single-application or the combined-application with other medicines including blood-fat reducing medicines to treat obesity, atherosclerosis and relevant diseases and/or illnesses.
CN102058694A Application of pharmaceutical composition consisting of amino acids and extracts The invention provides application of a pharmaceutical composition consisting of amino acids and extracts to preparing medicines for reinforcing memory, breeding hair and preventing alopecia, preventing and treating senile dementia, cerebral infarction and dizziness, head swell, headache and dim eyesight caused by long time use of computer or driving. The amino acids are ornithine and citrulline or salts thereof and the natural extracts are Chinese-date, gingkgo and ginseng extracts. The pharmaceutical composition can remarkably improve the content of superoxide dismutase and reduce the content of malondialdehyde in brain tissues of a mouse, reduce the damage of free radicals to the neural system, avoid and improve dementia and remarkably improve memory of animals with dysmnesia. The pharmaceutical composition can further relieve dizziness, head swell, headache and dim eyesight caused by long time use of computer or driving and has the function of breeding hair and preventing alopecia. The pharmaceutical composition can be prepared into granular formulation or oral liquid and is suitable for patients with dementia and cerebral infarction.
US7629155 foods and beverages containing 1,4-dihydroxy-2-naphthalene carboxylic acid or salts, used for improving intestinal flora, alleviating abdominal ailments caused by lactose intolerance and for preventing or treating metabolic bone diseases A composition containing 1,4-dihydroxy-2-naphthoic acid at a high concentration is obtained by intracellularly and extracellularly producing 1,4-dihydroxy-2-naphthoic acid using a bacterium belonging to the genus Propionibacterium and collecting it. This composition is efficacious in improving intestinal flora, alleviating abdominal ailments in association with the intake of milk, and preventing metabolic bone diseases.
WO2014063080A1 Treating polycystic kidney disease with hsp90 inhibitory compounds Provided are methods of treating polycystic kidney disease in a subject in need thereof, by administering to the subject in need thereof, an effective amount of a compound according to formula (I) or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods of treating polycystic kidney disease by a compound of formula (I) in combination with additional therapeutic agents.
EP1129089B1 Spiro-indolines as y5 receptor antagonists Compounds of general structural formula (I) such as that shown in structural formula (II) are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.
CA2609733C 6,7-unsaturated-7-carbamoyl-substituted morphinan derivative A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation. A compound represented by the formula (I): [Chemical formula I] (see formula I) wherein R1 and R2 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted aryl etc., R3 is hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted lower alkoxy etc., R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, cycloalkyl lower alkyl or lower alkenyl, or a pharmaceutically acceptably salt, or a solvate thereof is provided.
US20130012567 RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING CHEMICALLY MODIFIED SHORT INTERFERING NUCLEIC ACID (siNA) The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.
CN101214230A Asepsis patch for postoperative wound pain relieving The present invention discloses aseptic sticking membrane agent used for postoperation wound acesodyne, which consists of an anti-sticking layer, a drug-storing layer and a back lining layer. The drug-storing layer consists of framework material and microsphere loaded with local anesthetic, and the framework material is macromolecular polymer with film forming ability. The aseptic sticking membrane agent used for the postoperation wound acesodyne of the present invention can realize the uniform, lasting and slow release of the drug to achieve the lasting acesodyne effect, because the local anesthetic is wrapped inside the microsphere by the micro spheroidization technology. The aseptic sticking membrane agent used for the postoperation wound acesodyne of the present invention is used for the postoperation wound acesodyne, which can ensure that a patient does not have obvious painful feeling during the wound healing period.
CN101199528A Patch of carsick-prevention containing anisodine component The invention discloses a paster for treating motion sickness, belonging to drugs for treating nausea, motion sickness or vertigo. The preparation is composed of five layers: a protective layer, a mucilage layer, a controlled release film layer, a drug storage cavern layer and a backing layer. The components of the preparation are that: the drug storage cavern layer contains 10 percent to 50 percent of anisodine, 0 percent to 20 percent of transdermal enhancer, and the other component is water-soluble or water insoluble matrix; the mucilage layer contains 0 percent to 30 percent of the anisodine, 2 percent to 20 percent of the transdermal enhancer, and the other component is pressure sensitive adhesive; the backing layer is PET or non-woven fabric; the protective layer is PET film processed to antistick; and the controlled release film film is EVA polymer film. The total area of the paster is 1 square centimeters to 5 square centimeters, and each tablet contains the anisodine for 3 mg to 15 mg. The invention has obvious effect to treat carsickness, is convenient to be used, and does not have the disadvantages of the oral drugs; and the drug release in vitro of the invention reaches zero order rate process.
CN1565434A Orally administered Modafinil medicine compostion The invention discloses an orally administered Modafinil medicine compostion wherein no drinking water is needed during use for oral application. The composition can be orally disintegrated, dispersed or dissolved. The does type of the medicinal preparation include chewing tablet, buccal tablet, oral rapid collapsing tablet or oral instant tablet and oral glue.
US7029688 Methods and compositions to prevent formation of adhesions in biological tissues The invention discloses materials that adsorb readily to the surfaces of body tissues in situ and provide a steric barrier between such tissues, so that tissue adhesions, which typically form following surgical procedures, are minimized. These materials contain a polymer of hydrophilic molecules such as polyethylene glycol (PEG) bound to a polymer that spontaneously adsorbs to biological tissue such as phenylboronic acid (PBA). The PEG-PBA co-polymer can be formed in a variety of geometries. The materials can also be used to coat prosthetics and other implants.
WO2014082514A1 Method for initiating stem cells of mammals and use of chlorine dioxide in preparation of drug for initiating stem cells of mammals Provided in the present invention is a method for initiating the proliferation, migration and differentiation of stem cells in mammals, comprising the following steps: preparing a stem cell initiation agent containing chlorine dioxide and administering the stem cell initiation agent to target tissues of mammals, wherein an effective amount of chlorine dioxide is provided when administering the stem cell initiation agent to the target tissues of mammals. Also provided in the present invention is the use of chlorine dioxide in the preparation of a drug for initiating the proliferation, migration and differentiation of stem cells. The method of the present invention has a broad application range, and is suitable for various requirements of treating diseases using the tissue regeneration ability and immunity regulation ability of stem cells or prompting the initiation of the proliferation, migration and differentiation of stem cells in injured organs and organisms having regenerated tissues; furthermore, using the method of the present invention, the proliferation, migration and differentiation of stem cells can be initiated quickly and moderately; and the method has few side effects or no side effects, and can continuously be used for initiating the proliferation, migration and differentiation of stem cells.
EP1052975B1 Propofol composition containing sulfite Sterile pharmaceutical compositions for parenteral administration containing 2, 6-diisopropylphenol (propofol) are described for use as anesthetics. The compositions comprise an oil-in-water emulsion of propofol additionally comprising an amount of sulfite sufficient to prevent significant growth of microorganisms for at least 24 h after adventitious contamination.
US20090076009 Thiazole derivatives and their use as anti-tumour agents The invention concerns thiazole derivatives of Formula I or pharmaceutically-acceptable salts thereof, wherein each of R, Ring A, m, R1, R2 and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.
US20110190257 Bicyclic heterocycles as mek kinase inhibitors The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
CN101185628A Irinotecan sustained-release implant for treating solid tumor An irinotecan sustained release implant includes effective dose of anticancer irinotecan, sustained release excipients and a certain quantity of sustained release moderator. Solid tumors include pancreatic cancer, lung cancer, liver cancer, breast cancer, cerebroma, ovarian cancer, prostatic carcinoma, esophageal carcinoma, lymphadenoma, osteosarcoma and colorectal cancer. Sustained release excipients are mainly one or combination of copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly(L-lactide-co-ethyl phosphate), and poly (L-lactide-co-phosphoric acid propyl); in the process of decompression, irinotecanpto can be slowly and steadily released to local tumor, thus maintaining effective drug concentration of local tumor as well as significantly reducing overall toxic reaction. Being placed in local tumor, the sustained release implant not only reduces overall toxic reaction of irinotecan, but also selectively improves drug concentration in local tumor, enhancing the therapeutic effects of non-operative therapy such as chemotherapy drugs and radiotherapy.
WO2012068211A1 Tricyclic inhibitors of pro-matrix metalloproteinase activation This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
CN1500147B Improved gene expression Polynucleotides and vectors comprising an expressible nucleic acid flanked by a 5' extended methylation-free CpG island and a 3' selectable marker element are disclosed. Such polynucleotides and vectors provide a means for obtaining high levels of expression of the flanked expressible nucleic acid. Preferred embodiments include combinations of 5' extended methylation-free CpG islands and 3' antibiotic resistance genes.
US7009061 Diterpene compounds The present invention provides a novel diterpene compounds with antineoplastic activities. The novel diterpene compounds of the present invention are represented by the general formula (I). R1 to R6 in the formula represent an aliphatic group, or a radical represented by the general formula RCO—, wherein R represents an aliphatic, an aromatic or a heteroaromatic group. The compounds of the present invention may be prepared by extracting roots of Euphorbia kansui L. with an organic solvent such as chloroform, ethyl acetate and butanol. These extracted compounds may be used as starting materials for the preparation of the compounds represented by the general formula (I). The compounds of the present invention have antineoplastic activities, and therefore, useful as antineoplastic agents.
US20080160108 Method of treating muscular dystrophies with an inhibitor of histone deacetylase The present invention relates to the use of an inhibitor of histone deacetylase for preparing a drug for the treatment or prevention of a disease resulting from the deficiency of an adult gene in an individual by the re-expression of the homologous fetal gene. The invention concerns in particular the treatment of dystrophies such as Duchenne's dystrophy or Becker's dystrophy in which the defective adult gene is the dystrophin gene and the homologous fetal gene is the utrophin gene.
US20100113305 Oxazole and thiazole combinatorial libraries This invention provides a novel method for synthesizing an ensemble of peptides that allows for the generation of an unlimited number of antibiotic compounds. More specifically, the method comprises utilizes synthetic heterocyclic amino acids containing thaizole and/or oxazole as building blocks in a solid phase combinatorial synthesis to yield natural and unnatural antibiotic compounds.
CN102973585A Application of gentiopicroside in treatment of hyperuricemia The invention relates to an application of gentiopicroside or radix gentianae total glycosides containing the gentiopicroside more than 50% in preparation of medicines for treatment of hyperuricemia. The hyperuricemia is a common disease mainly caused by that long-term purine metabolic disturbance leads to increase of purine trione in blood and causes damage of tissue. The gentiopicroside can be extracted from large-leaved gentian or other plants of gentianaceae. According to the application, the mice serum uric acid is increased by two models respectively used for promoting uricolysis and inhibiting uricopoiesis, and the mice are treated by gentiopicroside powder injection by injection therapy and the gentiopicroside capsules by intragastric administration. Seven days later, the serum uric acid value is reduced remarkably, in comparison with a model group, t detection P is less than 0.05 (intragastric administration) and P is less than 0.01 (injection).
US7157570 Comprises nucleotide sequences coding enzymatic polypeptide for diagnosis, prognosis and treatment of cell proliferative disorders An isolated nucleic acid containing a human ribonucleotide reductase M2 subunit promoter sequence or genomic sequence. Also disclosed are methods of determining whether a subject is suffering from or at risk for developing a cell proliferation-associated disorder, identifying a compound for treating a cell proliferation-associated disorder, treating a cell proliferation-associated disorder, and developing a procedure for treating a cell proliferation-associated disorder.
CN101190230A Doxycycline hydrochloride chewable tablets for dog or cat The invention discloses a doxycycline hydrochloride chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the existing tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 10 to 30 percent of doxycycline hydrochloride.
CA2350894C Methods for preparing coated drug particles and pharmaceutical formulations thereof Disclosed are methods using pulsed laser ablation to prepare coated drug particles of uniform size and thickness. The coated drug particles ranged in size from several nanometers to several millimeters in diameter size, and were coated with organic polymer particle having average diameter sizes from about 1 to 50 nm. In illustrative embodiments, coated drug particles or drug delivery particles are disclosed comprising a biodegradable or biocompatible polymer coating having controlled thickness and controlled coating uniformity, that offer superior pharmaceutical properties for controlled delivery and increased bioavailability.
US20120003311 Method for controlled release of an acid-unstable physiologically active substance It is an object of the present invention, in the case of a controlled-release pharmaceutical composition, particularly a pulsed-release pharmaceutical composition, containing an acid-unstable physiologically active substance, to provide a pharmaceutical composition having little variation in dissolution lag time and high reliability of dissolution characteristics. The present invention discloses a controlled-release pharmaceutical composition comprising: 1) a core containing an acid-unstable physiologically active substance and a disintegrant; and 2) a release-controlling coating which covers the core, and which contains a water-insoluble polymer, an enteric polymer and a hydrophobic wax.
EP2189446B1 Novel 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy]-n'-(butoxycarbonyl)benzamidine crystals Type II crystals, type III crystals and type IV crystals of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy]-N'-(butoxycarbonyl)benzamidine are useful as the active ingredient of excellent antifungal agents.
CA2584075A1 Combined treatment with radiation and an epidermal growth factor receptor kinase inhibitor The present invention provides a method for manufacturing a medicament intended for treating tumors or tumor metastases in a patient, characterized in that a therapeutically effective amount of an EGFR kinase inhibitor and ionizing radiation is used, with or without additional agents or treatments, such as other anti-cancer drugs. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlotinib HCI (also known as Tarceva TM).
WO2005068467A1 Novel fused-ring compound The fused-ring compound of the formula shown below or an analogue or pharmaceutically acceptable salt thereof has the function of enhancing sugar transport and the function of depressing a blood sugar level and is useful for the prevention of and/or treatments for diabetes, etc. (In the formula, R is methoxy; Y is (2-thiazolyl)-2-ethylcarbonyl; R10 and R13 are hydrogen; and R11 and R12 are methyl.)
US20120053559 Treatment of Proliferative Diseases with Epothilone Derivatives and Radiation This invention relates to organic compounds of formula (I) in particular to pharmaceutical compositions for use in combination with ionizing radiation for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease.
US20100210624 Aryloxy- and heteroaryloxy-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin The aryloxy- and heteroaryloxy-substituted tetrahydrobenzazepine derivative compounds of the present invention are represented by formulae (I) (A-E) having the following structure where the carbon atom designated * is in the R or S configuration and the substituents X and R1-R9 are as defined herein.
CN103055141A Drug for treatment of gastric ulcer Relating to the technical field of Chinese and western medicines, the invention discloses a drug for treatment of gastric ulcer. The drug is prepared from the following Chinese and western medicinal raw materials by weight ratio:10-15 of Bletilla striata, 5-10 of membranes of hen eggs, 15-20 of cuttlebones, 1-5 of propolis, 1-10 of amoxicillin, and 1-5 of colloidal bismuth pectin. With the efficacy of nourishing yin and stomach, converging and relieving hyperacidity, killing bacteria and diminishing inflammation, promoting tissue regeneration and relieving pains, the drug provided in the invention has the advantages of strong efficacy, good curative effect, instant effect, short course of treatment, simple preparation, rich drug sources, and low cost.
CN101961406B Medicament for treating muscle and bone diseases caused by chronic infectious arthritis The invention discloses a medicament for treating muscle and bone diseases causes by chronic infectious arthritis, which is prepared into capsules from the raw materials including pangolin scales, earthworm, scorpio, rhizoma corydalis, Ukraine snake, suberect spatholobus stem, common monkshood mother root, kusnezoff monkshood root, ramulus et uncus uncariae, diclofenac sodium sustained release tablets, metoclopramide, noded pit viper and centipede. The medicament of the invention has small active ingredient loss and remarkable treatment effect and has the characteristics of addressing both the symptoms and root causes, avoiding side effects, effectively treating muscle and bone diseases causes by chronic infectious arthritis, along with low cost and short treatment course. When the medicament is used for treating muscle and bone diseases, such as osteoproliferation, protrusion of lumbar vertebral disc, cervical spondylosis and scapulohumeral periarthritis, caused by chronic infectiousarthritis in clinic, the effectiveness of the medicament is up to 90 percent.
CN103655562A Stable milrinone medicament composition for injection The invention discloses a novel stable milrinone medicament composition for treating congestive heart-failure, and a preparation method of the milrinone medicament composition. The milrinone medicament composition consists of milrinone, cysteine hydrochloride, sodium calcium edentate and water for injection. The medicament composition disclosed by the invention is high in stability, simple in preparation process, convenient in clinical application and easy to achieve industrial implementation.
CN101522688B Novel dithiolopyrrolones and their therapeutical applications The present invention provides dithiolopyrrolone compounds of the general formula I, and their salts, wherein A is sulfur or carbon, and R1, R2, and R3 are selected from groups defined herein, and wherein when A is sulfur, then B is oxygen, and n = 1 or 2, and when A is carbon, then B is oxygen or sulfur, and n = 1. The compounds are useful for the prevention and treatment of microbial infections such as HIV infection, and for the treatment of blood disorders, such as neutropenia. In particular, the compounds are useful for the manufacture of medicaments for increasing white blood cells.
CN101288660B Levonorgestrel drop pills preparation method The invention provides a Levonorgestrel pill and a preparation method thereof. The Levonorgestrel pill consists of a pill core and a coating layer, wherein, the pill core comprises Levonorgestrel active ingredient, carrier used as dispersant and surface active agent with a weight ratio of 1: 10-60: 1-10; the coating material used by the coating layer consists of coating powders and correctives. The coating powders adopt gastric solubility film coating powders, the dosage of which is 2-6 percent (w/w) of the total amount of the Levonorgestrel pill; the dosage of the correctives is 0.1-2 percent (w/w) of the total amount of the Levonorgestrel pill. The preparation method of the Levonorgestrel pill is that the Levonorgestrel raw material is micronized to a grain diameter of less than 20 Mu m; in the preparation process, main medicine is evenly dispersed in the carrier to form a solid dispersoid, thus improving the drug water solubility, increasing the drug dissolution rate and bioavailability and more effectively playing a curative role.
CN102357223A Medicine for curing acute soft tissue injury and preparation method thereof The invention discloses a medicine for curing acute soft tissue injury and a preparation method thereof. Red flower, long pepper, asarum, semen brassicae, galangal, dragon's blood, rhizoma corydalis, raw frankincense, raw myrrh, camphor and borneol are used cooperatively and have the functions of promoting blood circulation, removing blood stasis, eliminating swelling and relieving pain. The medicine has obvious curative effect and does not have adverse effects.
CN103099792A Preparation method of IV crystal linezolid tablets having high drug loading capacity and capable of quickly dissolving The invention discloses a preparation method of IV crystal linezolid tablets having high drug loading capacity and capable of quickly dissolving. The preparation method comprises the following steps of preprocessing, premixing, mixing, granulating, drying, arranging granulates, centrally controlling, tabletting and coating. According to the preparation method, corn starch and silica are matched with each other, therefore, the tablets with hardness more than 30kg can be quickly cracked, and the in-vitro dissolution similarity ranging from 50 to 100 with respect to a referred product, as well as high drug loading capacity, can be realized.
WO2008135232A1 Use and compositions of purine derivatives for the treatment of proliferative disorders The present invention relates to inhibitors of Aurora A, Aurora B, Aurora C, CHK2, JNK1 α1, JNK3 and abl kinase and their biological applications. In particular, the invention relates to substituted purines and purine derivatives and compositions thereof featuring antiproliferative properties which are useful in the treatment of proliferative disorders such as cancer, leukemia, psoriasis and the like.
US20120220576 Novel Heterocyclic Derivatives The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
CN1634120A Dripping pills of grifola umbellata polysaccharide The invention discloses a pharmaceutical composition for treating hepatitis B and has anticancer action, more specifically an oral preparation with polyporus umbellatus polysaccharose as the active component, i.e. a dripping pill of grifola umbellata polysaccharide, which also comprises a finite proportion of medicinal carrying agent as the substrate.
CN103284948A Preparation and application of polymer composition loaded with sirolimus compound or its derivative The invention relates to a polymer composition loaded with a sirolimus compound or its derivative. The composition can have diversified forms. A necessary link includes preparing the sirolimus compound or its derivative and a polymer carrier into a micelle. Then according to needs, the micelle can be further prepared into a freeze-dried composition by a freeze-drying technology, or the micelle and other polymer and carrier can be prepared into a solid or semi-solid preparation. The polymer composition can be used for treating tumors, reducing rejection reactions after organ and tissue transplantation, promoting cell regeneration and repair, preventing excessive scar tissue growth after injury and preventing vascular restenosis and blood coagulation embolism, treating or inhibiting autoimmune diseases, and treating or inhibiting inflammation, etc.
US20100010034 Crth2 antagonists The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: [3-(2,4-dichlorophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(2-fluoro-4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methanesulfonyl-2-trifluoromethylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, (R)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, [3-(4-ethanesulfonylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, (S)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, ethanesulfonylaminobenzenesulfonyl)-6-fluoro-2-methyiindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(2-chloro-4-methanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(4-methanesulfonylbenzyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-chlorobenzyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(6-fluoroquinolin-2-yl-methyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-bromophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, and [3-(4-cyclopropylsulfamoylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid.
WO2010103429A1 1,1-(Dimethyl-Ethylamino)-2-Hydroxy-Propoxy]-Ethyl}-3-Methyl-Biphenyl-4- Carboxylic Acid Derivatives As Calcium Receptor Antagonists The present invention is directed to novel 1,1 -(dimethyl-ethylamino)-2- hydroxy-propoxy]-ethyl}-3-methyl-biphenyl-4-carboxylic acid derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variable R1 is as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.
US20100047332 Treatments for burns using thyroid hormone compound in a human A topical preparation for treating first and second degree burns includes TriAc. The topical preparation preferably includes less than 10 mg of TriAc per 100 ml of pharmaceutical excipient base. In another embodiment, a topical preparation includes TriAc for decreasing cellulite. In this embodiment, the topical preparation is preferably applied only before exercise. In a preferred embodiment, the preparation is applied only intermittently, preferably no more than three times a week, or in amounts sufficient to not downregulate receptor number and become inefficacious.
CN101322574A Powdered beverage composition The invention relates to a cold water soluble, low calorie, low net carbohydrate powdered beverage composition containing protein and fiber suitable for reconstitution with water or aqueous based liquids. More specifically, the present invention relates to a cold water soluble, low calorie, low net carbohydrate powdered beverage composition comprising (1) a protein component, (2) a soluble fiber component, and (3) an optional high intensity sweetener component, wherein the soluble fiber component increases the flowability and cold water solubility of the powdered beverage composition.
CN101591314A Ophiobolin di-sesquiterpene compound and preparation method and application thereof The invention relates to an ophiobolin di-sesquiterpene compound and a preparation method and application thereof. The preparation method produces the compound of novel structure by using Aspergillus ustus 094102 (culture collection number: CCTCC M 208153) separated from soil samples of the root system of mangrove plant Bruguiera gymnorrhiza in Touyuan town, Wenchang. Experiments show that the ophiobolin di-sesquiterpene compound can be used as cell proliferation restraining agent or antitumor agent.
CN101311273A Biosynthesis gamma-aminobutyric acid preparation and method for preparing same The invention relates to a biosynthesized gamma-aminobutyric acid preparation. By weight percentage, the product comprises 5 percent to 60 percent of gamma-aminobutyric acid. The preparation method of the biosynthesized gamma-aminobutyric acid preparation includes the following steps: first, streptococcus lactis strains are inoculated to a seed medium for fermentation composed of glucose, corn steep powder, defatted soybean flour and monosodium glutamate, thus forming fermentation broth; the fermentation broth is drained into a high speed centrifuge to form clear liquid centrifugally; the clear liquid is added with 250 mg/L chitosan at the temperature of 40 DEG C, and stirred for flocculation; the flocculated fermentation broth to be filtered enters a plate-and-frame filter, thus obtaining filtered clear liquid; the filtered clear liquid passes a cationic resin exchange bed for ion exchange; when ion exchange resins are saturated, the liquid is eluted by deionized water to elute all the glutamate; ammonia is used for eluting the liquid and extracting the gamma-aminobutyric acid. The method realizes large scale production of functional food factor GABA, so the method adapts to the production and processing of food with various forms and specifications as well as GABA products of nutritional foods.
US20110028462 Niacin Receptor Agonists, compositions Containing Such Compounds and Methods of Treatment A method of treating atherosclerosis and related conditions using compounds of formula I: as well as pharmaceutically acceptable salts and solvates is disclosed. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels.
CN101863890A Imidazole alkaloid extracted from Echinogorgia pseudossapo and preparation method and application thereof The invention relates to an imidazole alkaloid extracted from Echinogorgia pseudossapo and a preparation method and application thereof. The imidazole alkaloid is characterized in that the structure of the alkaloid is expressed in the following general formula (1), wherein R=-OCH2CH2CH2CH3 or -CH2CH2CH2CH2CH2COOH or -CH2CH=CHCH2CH2CH2COOH, and a double-bond of the -CH2CH=CHCH2CH2CH2COOH has transconfiguration. The alkaloid is prepared by the following steps of: extracting Echinogorgia pseudossapo by an organic solvent to obtain a crude extract; extracting sequentially by chloroform or ethyl acetate or n-butyl alcohol; carrying out silica gel column chromatography on the obtained n-butyl alcohol layer; taking a component which can be expanded by a mixing solvent of chloroform and methanol with the volume ratio of 10:1 and presents a plurality of blue fluorescent spots under an ultraviolet lamp for further carrying out normal pressure silica gel column chromatography to obtain three small components; and respectively carrying out normal pressure silica gel column chromatography and high performance liquid chromatography column separation to obtain the three compounds with the general formula (1). The alkaloid can be used for resisting a herpes simplex virus I and a respiratory syncytial virus.
CN101095714A Medicine for treating skin scald and burn and method for preparing the same The invention discloses a medicament for treating skin burns and scalds, which is prepared from gypsum, astragalus root, borax, frankincense, ginseng, boneol, dragon's bone and sesame oil through frying and grinding.
CN102138935B Melanterite-containing medicinal composition and preparation method thereof The invention relates to a medicinal composition for promoting hemopoiesis, which contains hemopoietic stem cells and melanterite, wherein the hemopoietic stem cells are preferably cells into which expression vector carrying cell factor genes are transferred. The invention also relates to a preparation method of the medicinal composition and application of the medicinal composition in the preparation of medicaments for treating damaged hematopoietic functions, wherein the hemopoietic stem cells and the melanterite have the effect of promoting the hemopoiesis synergistically.
CN103421069A Fulvestrant phosphate derivative and preparation method and application thereof The invention discloses a fulvestrant phosphate derivative and a preparation method and application thereof, and aims to solve the problem in the prior that the fulvestrant drug substance is poor in ordinary temperature stability. The fulvestrant phosphate derivative can be used for preparing medicines capable of preventing and treating breast cancers, and is a compound with a novel structure and fulvestrant mother ring 3-phenolic hydroxyl is carried out phosphate. According to a method for fulvestrant phosphate phosphate, the material is easy to obtain, the synthesis method is simple, and the purification manner is simple, convenient and fast. Moreover, the derivative provided by the invention is higher in stability compared with an original drug; under the catalysis of the cytochrome P 450 enzyme CYP3A4 and alkaline phosphatase, the original drug can be released, so that the kind of compound has a broad application prospect in preparing the medicines capable of preventing and treating breast cancers. The derivative has the structural formula as shown in the description.
CN103193754A 7-acyl-15-oxo-spiraea lactone derivative as well as preparation method and applications thereof The invention provides a 7-acyl-15-oxo-spiraea lactone derivative which is a medicinal composition of medicinal active ingredients, a preparation method of the derivative, an application of the derivative in preparation of medicaments for resisting hepatitis C virus, and an application of the derivative in preparation of antivirus medicaments. In the process of studying plant antitumor natural products, 7-acyl-15-oxo-spiraea lactone is discovered to have activity of resisting various tumor cell strains, and most derivatives are stronger than a primer 15-oxo-spiraea lactone (1). The 7-acyl-15-oxo-spiraea lactone derivative is subjected to an activity test for inhibiting a Wnt signal channel, and the antitumor activity of the 7-acyl-15-oxo-spiraea lactone derivative is discovered to be in positive correlation with the activity of the 7-acyl-15-oxo-spiraea lactone derivative for inhibiting the Wnt signal channel.
WO2010017633A1 Use of nitric oxide The present invention relates to uses, compositions, devices, and methods involving the utilisation of nitric oxide to hinder, impede, inhibit, or prevent transmission of infectious viral particles to host cells.
WO2011150457A3 Haematopoietic-prostaglandin d2 synthase inhibitors The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D2 synthase (H-PGDS), to compositions containing them and to their use in treating or preventing conditions and diseases associated with H-PGDS, such as allergies and inflammation.
CN1879831A Bacteriostatic externally applied preparation for treating gynecological inflammation and method for preparing same The invention relates to a Chinese pharmaceutical composition for treating gynaecologic inflammation and process for preparation, wherein the composition is prepared from flavescent sophora root, rhubarb horsetails, cnidium fruit, corktree bark, poria cocos, Chinese dittany bark, roor of sessile stemona, wild chrysanthemum flower, Senecio scandens, zanthoxylum piperitum, carpesium fruit, evodia rutaecarpa, cortex pseudolaricis, gentian root, black catechu, dahurian angelica root, broom cypress fruit, dried alum, borax, metronidazole and auxiliary materials.
CN101530583A Composition and preparation method of thin paste for treating pain and numbness The invention relates to a composition and preparation method of a thin paste for treating pain and numbness. The method comprises the steps of: taking raw materials of long pepper, unprocessed radix aconite, unprocessed radix aconiti kusnezoffii, raw pinellia ternate, arisacma consanguineum schott, black pepper, asarum, angelica, raw frankincense, myrrh, speranskia tuberculata, strychnos, ligusticum wallichii, Chinese clematis, and radix angelicae pubescentis, later carrying out cleaning and airing, and then adding ethanol, carrying out impregnation at normal temperature and concentration by heating; taking and adding 654-II and chlorpheniramine to a container with alcohol for soaking for 2 days, heating for concentration, and then mixing and stirring the two types of soaking liquids after concentration with rosin which takes liquid shape by heating, and finally spreading paste to obtain the thin paste. Medicaments prepared by the method has the functions of relaxing muscle and activating blood, stopping pain and removing numbness, and particularly has very significant therapeutic effect on the hand-foot-waist-leg pain and numbness caused by various reasons such as cervical spondylosis, lumbar disc herniation, rheumatic and rheumatoid arthritis, and the like.
CN101966170B Compound lidocaine paster and preparation method thereof The invention relates to a compound lidocaine paster and a preparation method thereof. The compound lidocaine paster comprises a seal cap and a pasting part, wherein the pasting part comprises an annular foam tape, a water absorbing fiber plate and a gasket; the water absorbing fiber plate is immersed with compound lidocaine emulsion; the water absorbing fiber plate is sealed in mesopores of the annular foam tape between the gasket and the cap; the inner surface of the gasket is heat-sealed with the outer surface of the annular foam tape into a whole, and the gasket is large enough to cover the mesopores of the annular foam tape; the water absorbing fiber plate is attached to the inner surface of the gasket and is arranged in the mesopores of the annular foam tape; the water absorbing fiber plate is stored in a sealed manner by the heat seal of the gasket and an annular pressure tank; and a piece of self-adhesive paper in the annular foam tape and the seal cap are pressed and heat-sealed, and the shape of the seal cap is matched with the annular foam tape. The compound lidocaine paster can be used conveniently by the following steps of: firstly removing the cap, and then directly pasting the pasting part on a skin surface needed to be narcotized. The compound lidocaine paster has the advantages of simple structure and obvious curative effect, and is suitable for local skin anesthesia in needle penetration and small operation of intact skin surgery.
US20120244193 Passive solid tumor targeting anticancer prodrug and preparation method thereof The invention relates to a passive solid tumor-targeted anticancer prodrug and a preparation method thereof, belonging to the field of antitumor drugs. The preparation method includes the following steps: reacting low molecular weight pectin with Mw of 5,000-45,000 with doxorubicin to obtain a pectin-doxorubicin conjugate with Mw of 100,000-1,000,000, preparing the conjugate into a suspension, and treating the suspension in an ultra-high pressure nano homogenizer to obtain the passive solid tumor-targeted anticancer prodrug with particle size of 100 nm-200 nm and melting point of 220-245°, wherein the pectin and doxorubicin are linked by an amide bond, and the pectin is linked by an ester bond formed by condensing carboxyl groups and hydroxyl groups of pectin molecules. Cell inhibition rate of the anticancer prodrug for humanized lung cancer cells NCI-H446 and A549 is equivalent to that of doxorubicin hydrochloride. In the efficacy research of melanoma B16 pulmonary metastasis model mice, the life span of tumor-bearing mice is 42.3±12.4 days, which is remarkably higher than that of the doxorubicin hydrochloride group (23.1±10.2 days).
CA2398353C Anticancer compound and enantiomer separation method useful for synthesizing said compound The present invention relates to the compound (+)-6-[amino-(6-chloro-pyridin-3yl)-(3-methyl-3H-imidazol-4-yl)--methyl]-4-(3-chloro-phenyl)-1-cyclopropylmethyl-1H-quinolin-2-one, pharmaceutically acceptable salts and solvates thereof, pro-drugs thereof, and to the use of said compound for inhibiting abnormal cell growth, including cancer, in mammals. The invention also relates to methods useful in synthesizing the aforementioned compound.
CN1569001A Dripping pills of doxepin hydrochloride and its preparation The invention discloses a doxepin hydrochloride drop pill prepared through ultramicro disintegration and drop pills manufacturing technique, which has the advantages of improving collapse and dissolving speed, dissolving out speed and degree, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use. It has good compliance, thus is especially suitable for children, the elderly, bedridden patients and dysphagia patients.
CA2295792C A crystalline dibenzothiazepine derivative and its use as an antipsychotic agent Crystalline 11-(4-[2(2-hydroxyethoxy) ethyl]-1-piperazinyl)-dibenzo[b,f] [1,4]thiazepine (I) may be prepared by crystallising 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine from a non-aromatic solvent such as ethyl acetate, isobutyl acetate, methyl iso-butylketone or methyl tert-butyl ether, preferably in the absence of water. The crystalline material produced may be converted into a pharmaceutically acceptable salt such as a fumarate. The crystalline 11-(4-[2-(2-hydrox-yethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine may be used to treat psychoses.
US20110306018 Methods For Improving Pregnancy Outcomes The present invention relates to promoting whole body health in humans and animals by using topical oral compositions comprising a safe and effective amount of an antimicrobial agent in admixture with a pharmaceutically acceptable carrier, said compositions being effective in controlling bacterial-mediated diseases and conditions present in the oral cavity and in inhibiting the spread into the bloodstream of pathogenic oral bacteria, associated bacterial toxins and endotoxins, and resultant inflammatory cytokines and mediators. The present invention also encompasses methods of use of these compositions by topically applying to the oral cavity, a safe and effective amount of an antimicrobial agent to promote and/or enhance whole body health in humans and other animals.
EP1417955B1 Humectant and cosmetics and external preparations containing the same An object of the present invention is to provide a humectant which is excellent in moisture retaining properties and stability at high temperature above 40 DEG C, and a cosmetic and an external agent comprising the same. In order to achieve the object, the present invention provides a humectant comprising, a component A: an ester compound comprising at least one of glycerin and a condensate of the same, a straight chain saturated fatty acid having 16-28 carbons, and an aliphatic dibasic acid having 16-28 carbons, more than half of the hydroxyl groups of at least one of the glycerin and the condensate of the same remaining as hydroxyl groups in the ester compound; a component B: a dihydric water soluble alcohol; and a component C: a polyhydric water soluble alcohol which is trihydric or above. Further, the present invention provides a cosmetic and an external agent comprising the humectant.
CN102133386A Tuber pinellia and dried ginger composition, preparation method thereof and application of tuber pinellia and dried ginger composition in preparation of attenuated synergistic medicaments in cancer radiotherapy and chemotherapy The invention relates to a natural pharmaceutical composition, a preparation method thereof and an application of the natural pharmaceutical composition in preparation of attenuated synergistic medicaments in cancer radiotherapy and chemotherapy. The natural pharmaceutical composition is prepared from extract obtained by concentrating tuber pinellia and dried ginger powder, gingerol, tuber pinellia alkaloid and tuber pinellia polysaccharide according to the ratios of (3-8):(2-6):(1-5):(2-7). The composition has an excellent effect on treating emesis and other side effects caused by cancer radiotherapy and chemotherapy, and can simultaneously play a role in inhibiting tumors.
CN101862416A Itching-relieving and ringworm-eliminating liquid and preparation process thereof The invention provides itching-relieving and ringworm-eliminating liquid and a preparation process thereof. The itching-relieving and ringworm-eliminating liquid comprises a lipid phase and a water phase, wherein the lipid phase comprises the following components in percentage by mass: 1 to 3 percent of natural menthol, 0.2 to 3 percent of Australian tea-plant essential oil and 0.1 to 1 percent of propolis; and the water phase comprises the following components in percentage by mass: 0.1 to 1.5 percent of thyme, 0.1 to 1.5 percent of folium eucalypti, 0.1 to 1.5 percent of white willow, 0.1 to 1.5 percent of bletilla hyacinthina reichb, 0.1 to 1.5 percent of cortex pseudolaricis extract, 0.1 to 1.5 percent of allantoin and 0.1 to 1.5 percent of nanometer sulphur. The itching-relieving and ringworm-eliminating liquid is used for treating beriberi (athlete's foot and tinea pedis), foot odor, foot itching, hand and foot ringworm and the like, can relieve pain and itching immediately, ensures medicament action lasts for over 24 hours, prevents the second infection and cross infection of foot fungi effectively and avoids the relapse of the beriberi.
US20100286121 Water-Immiscible Materials as Vehicles for Drug Delivery A pharmaceutical composition includes at least one pharmaceutical component and at least one water-immiscible material. The pharmaceutical component is more soluble in the water-immiscible material than in water. The pharmaceutical composition is suitable for ocular administration.
WO2014164968A1 Novel compounds for the treatment of hepatitis c The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. Formula (I). I
WO2011079766A1 Aripiprazole solid preparation and the production method thereof A production method of an aripiprazole solid preparation and the preparation produced by the method are disclosed. The method comprises: dissolving aripiprazole in the acid solution containing acidifying agent to obtain an acid liquid of the medicine; later, homogeneously mixing adjuvants and the acid liquid of the medicine, carrying out wet granulation.
WO2009049406A1 Use of ps20 /wfdc1 and interferons to diagnose, monitor and treat viral diseases Methods for detecting, diagnosing or monitoring viral diseases in a subject are described comprising measuring ps20 polypeptides or ps20 polynucleotides and interferons and interferon polynucleotides in a sample from the subject. The invention also contemplates therapeutic applications for viral diseases employing modulators of ps20 polypeptides and ps20 polynucleotides in combination with interferon or interferon polynucleotides.
US20050019854 Analyzing insulin response; solid phase synthesis; for treatment of prediabetes, hyperinsulinemia, and type II diabetes; kits The invention concerns a detection procedure for compounds modulating the complexation between neuronal nitric oxide synthase protein (nNOS) or one of its variants and the protein inhibitor of neuronal nitric oxide synthase (PIN), in which: a mixture of the said compound, the PIN and the nNOS or one of its variants is incubated, significant variation in the quantity of complex formed between the PIN and the nNOS or one of its variants with respect to a control value is detected, when there is significant variation as defined above, it is concluded that there is binding between the said compound and the PIN, or between the said compound and the nNOS or one of its variants, leading to modulation of the complexation between the PIN and nNOS or one of its variants.
CN1943582A Foscarnet sodium composition The invention provides a new clinical uses for treatment of Th1/Th2 balance disorder by medicine composition wherein foscarnet sodium as active component, particularly use for Th1/Th2 balance disorder caused by in treatment of hepatitis b virus.
CN103497181A Benzoperhydroazepinone compounds as glycogen phosphorylase inhibitors as well as preparation method and medical application thereof The invention relates to the pharmaceutical chemistry field and specifically relates to novel benzoperhydroazepinone derivatives (I) as well as a preparation method and a medical application thereof. The compounds have glycogen phosphorylase inhibiting effect, and can be used for preparing anti-diabetic and anti-diabetic complication drugs, anti-cerebral ischemia drugs, anti-cardiovascular disease drugs, lipid-lowering drugs, weight-reducing drugs, anti-atherosclerotic drugs, drugs for treating metabolic syndromes or antitumor drugs. The invention further relates to a preparation method of the compounds as well as a pharmaceutical preparation containing the compounds.
CN101352499A Nidaodier tablet medicine The invention relates to the medical therapy technical field of a Nidaodier tablet and belongs to the technical field only for radically curing various cancers. The invention has the functions of clearing away heat and toxic materials, diminishing inflammation, alleviating pains, promoting digestion and absorption, and activating utilization. The Nidaodier tablet can firstly enhance the body resistance, then alleviate the symptoms and systematically target the lesions of cancers, thus achieving the functions of diagnosis and treatment; coordinating with the body of a patient, the invention can indirectly dissolve tumor and directly guarantee the normal growth of white blood cells. Thereof, the healing result can be directly witnessed as long as diagnosis and treatment are carried out. The results show that patients with various cancers can be cured and survive healthily as long as the patients receive the 'Nidaodier' diagnosis and treatment of the invention in time; and no sequelae is technically left over.
WO2007134709A1 5-iodotetrazoles for use as antimycotic 5-Iodotetrazoles of the formula (I) in which R1 has the meaning given in the description are exceptionally suitable for use as medicaments, in particular for the combating/prophylaxis of mycoses in humans and mammals.
US20110311591 Antimicrobial Coating A substrate (100) comprising a sol-gel derived coating (101). The coating, is chemically bonded to the substrate (100) and is derived from a polysiloxane to form a network of silicon-carbon and silicon-oxygen bonds. An antimicrobial is releasably captured within the network and is capable of defusing from the coating in vivo in response to introduction of a fluid into the coating.
US20080319024 Rosiglitazone Phosphate and Polymorphic Forms The present invention relates to 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione phosphate, a novel salt of rosiglitazone and to novel polymorphic forms thereof. The invention is also directed to processes for preparation of rosiglitazone phosphate and its polymorphs. The compounds of the invention are useful for treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof.
CN100998871A Chiral medicine D-antothenic acid intercalation hydrotalcite and its preparation method A chiral medicine D-pantothenic acid intercalated hydrotalcite with high thermal stability and optical stability and a certain slow-release nature has a chemical formula: (Mn+)1-x(M3+)x(OH)a(D-C9H16NO5)6.mH2O. Its preparing process includes such steps as preparing the precursor of hydrotalcite by single-drop codeposition method, and ion exchange reaction with the calcium D-pantothenate solution in ultrasonic generator.
US7473704 Cyclohexyl prostaglandin analogs as EP4-receptor agonists The invention relates to the use of novel cyclohexyl analogues of E-type prostaglandins as EP4 agonists, in general, and, in particular as ocular hypotensives. The cyclohexyl analogues used in accordance with the invention are represented by the following formula I: wherein the wavy segments represent α or β bond, dashed line represents the presence or absence of a bond W, Y, Z, R, R1, R2 and R3 are as defined in the specification.
US20110046209 RNA-Induced Translational Silencing and Cellular Apoptosis The invention is directed to RNA molecules that can be used to inhibit protein synthesis and to induce cells to undergo apoptosis. It also includes pharmaceutical compositions containing the RNAs that can be used in treating or preventing tumors; abnormal dermatological growths and viral infections.
EP1875925A1 Preventive or remedy for bowel disease [Problem] To provide a preventive or a remedy for various diarrheas caused by inflammatory colitis, irritable bowel syndrome and other factors. [Means for Solution] It was found for the first time that CRAC/SOC channels play a physiologically important role in water secretion or absorption in gastrointestinal epithelia cells and a CRAC/SOC channel inhibitor is useful for preventing and treating diarrhea caused by various factors, and a preventive and a remedy for diarrhea comprising a compound inhibiting the calcium-release-activated calcium channels as an active ingredient, particular a remedy for diarrheal symptoms associated with inflammatory bowel diseases and a remedy for irritable bowel syndrome are provided.
WO2008141021A1 Deuterated derivatives of tetrahydrotriazolopyrazine compounds and their use as dpp-iv inhibitors This invention relates to novel substituted tetrahydrotriazolopyrazines of formula (I) and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an enzyme inhibitor of dipeptidyl -peptidase IV (DPP-IV) wherein each Y variable is independently hydrogen or deuterium; each Z variable is independently hydrogen or deuterium; R1 is a phenyl ring substituted with zero to three fluoro and zero to five deuterium groups; R2 is CF3, Cl, CH2D, CHD2, or CD3; with the proviso that if each Y and Z variable is hydrogen and R1 has zero deuterium, then R2 comprises a deuterium atom.
EP2142511A2 Heterocyclyl-substituted-tetrahydro-naphthalen-amine derivatives, their preparation and use as medicaments The present invention relates to heterocyclyl-substituted-tetrahydro-naphtalen-amine compounds of general formula (I) methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals, mediated by the 5-HT7 receptor affinity.
CN103463028A Application of Lycojaponicumin A in anti-influenza A virus medicaments The invention discloses an application of Lycojaponicumin A in preparation of anti-influenza A virus medicaments. Experiments prove that the Lycojaponicumin A has a prominent inhibiting effect on influenza A viruses fluA, which hints that the Lycojaponicumin A has a potential application value in the field of treatment of influenza A virus infected diseases. The application of the Lycojaponicumin A in preparation of the medicaments for treating influenza virus infection is made public for the first time, the skeleton type is completely novel, and the Lycojaponicumin A has an unexpectedly strong influenza virus inhibiting activity, so the probability that other compounds give any revelation does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in prevention and treatment of the influenza virus infection.
EP1317489B1 A mixture of non-sulfated fucose-based oligosaccharides, a cosmetic or pharmaceutical composition comprising said mixture and its use in cosmetics or pharmacy The present invention relates to a mixture of non-sulfated fucose-based oligosaccharides, characterized in that it comprises oligosaccharides of less than 13 saccharide units, comprising at least one fucose unit in a non-reducing end position, and in that at least it is capable of being obtained by means of a process that comprises at least one step of degradation of a polysaccharide from a microorganism of the gender Klebsiella pneumoiae subsp. pneumoniae. This new mixture presents significant activities on different components of the skin, providing a clearly visible anti-aging result, specially by an excellent thickening of the skin.
US6916808 2-thio-4h-3, 1-benzoxazin-4-one derivatives for use as enzyme inhibitors The use of a compound, comprising formula (I) or a salt, ester, amide of prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is an optionally substituted 6-membered aromatic or heteroaromatic ring; and R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups
WO2009079693A1 Design and selection of medicaments that modulate the function and activity of interleukin 13 The present invention relates generally to the field of medicaments in the form of therapeutic molecules including inflammatory modulators and their design and selection. More specifically, the present invention relates to a target site on Interleukin 13 (IL- 13) by which a GAG molecule or polyanionic glycocoηjugate or anionic polysaccharide modulates IL-13 activity or function, said target site selected from the list consisting of amino acids located in the AB loops and/or helix D of human IL- 13 or its homolog or derivative, and the use of said IL- 13 target site to design a medicament for modulating physiological processes. Therapeutic and prophylactic compositions comprising the designed medicaments are also contemplated.
US20080207597 Homopiperazine compounds that inhibit ribosomal frameshifting by binding to rna pseudoknot structure of sars coronavirus Provided is a homopiperazine compound for inhibiting ribosomal frameshifting by binding to an RNA pseudoknot structure of SARS coronavirus. Particularly, the present invention provides a pharmaceutical composition for inhibiting synthesis of protein induced by −1 frameshifting by binding to an RNA pseudoknot structure specifically existing in SARS coronavirus. The composition includes a therapeutically effective amount of homopiperazine compound of following chemical formula 1 or a pharmaceutically accepted salt thereof, and a pharmaceutically accepted carrier or excipient.
CA2119261C Novel sidechain-bearing taxanes and intermediates thereof Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided. Methods of the invention are used for the preparation of compounds of the following formulas:
EP2776410A1 Disubstituted triazine dimers for treatment and/or prevention of infectious diseases The present invention relates to novel compounds (I) containing two disubstituted triazine rings covalently linked by an organic linker, thereby creating dimers. These compounds show activity against the causative infective agents of infectious diseases such as African trypanosomiasis, Chagas disease, Leishmaniasis, Malaria and HIV. The invention further relates to the prevention and/or treatment of these diseases.
CN101439042B Anti-tumor use of isoamylene flavonoid glycoside The invention discloses an isopentenyl flavonoid glycoside compound or an antitumor usage of solvate, stereoisomer, tautomer and prodrug thereof. Researches show that the compound remarkably inhibits various tumor diseases and particularly inhibits colon cancer, breast cancer, leucocythemia, lung cancer, liver cancer, etc.
US20130216585 Composition and methods for quenching free radicals and modulating inflammation Compositions and methods useful in quenching free radicals, the compositions including dihydroquercetin, vitamin C and Arabinogalactan, specifically, larch arabinogalactan, effective to enhance the immune modulating properties of Larch Arabinogalactan by quenching the free radicals that initiate a cascade of oxidative stress and inflammation.
WO2012093192A1 Coly-mycin derivatives The present invention relates to the isolation, cloning and sequencing of the group of genes involved in the biosynthesis of coly-mycin by Streptomyces spp. CS40, and to the use of said genes to increase the production of coly-mycin and/or associated analogous compounds or derivatives by means of productive strains. Said compounds produced in the present invention can be used to treat several diseases, such as cancer, neuro-degenerative diseases and infectious diseases.
US20100068297 Antimicrobial Composition Disclosed herein are antimicrobial compositions comprising an effective concentration of a metal salt combined with a plant extract. In some embodiments the composition comprises a copper salt and/or an iron salt and/or a nickel salt and/or a cobalt salt; and an extract of a plant selected from a group consisting of Punka granatum, Viburnum plicatum, Camellia sinensis, and Acer spp. The invention extends to uses of such compositions as medicaments, and to methods of treating microbial infections. The invention extends to methods for preventing microbial infections by coating objects and surfaces with the compositions.
US8597683 Modified release tranexamic acid formulation A modified release dosage form for the oral administration of tranexamic acid.
US20090169616 Formulation and method for the release of paroxetine in the large intestine The present invention provides a delayed and/or controlled release formulation of paroxetine or a pharmaceutically acceptable salt thereof that is formulated to release a substantial portion of the active ingredient (e.g., paroxetine) in the large intestine of an individual in need thereof. In one embodiment, the present invention provides a controlled release paroxetine composition comprising paroxetine or a pharmaceutically acceptable salt thereof, in a controlled release swallow pharmaceutical formulation, that upon administration, releases the paroxetine substantially in the large intestine. For example, the controlled release paroxetine formulation may be formulated to release greater than about 50% of the paroxetine in the large intestine.
CN102972753A Health product having functions of yang strengthening and kidney invigorating The present invention discloses a health product having functions of yang strengthening and kidney invigorating. The health product is prepared from the following raw materials, by weight, 20-40 parts of medlar, 5-15 parts of common yam rhizome, 4-12 parts of dodder, 4-8 parts of cartialgenous, 4-16 parts of epimedium, 3-9 parts of actinolite, and 5-20 parts of medicinal morinda root. The health product having functions of yang strengthening and kidney invigorating has effects of kidney warming and yang strengthening, body constitution enhancement, impotence and kidney asthenia symptom release, and sexual function improvement, and has characteristics of safe taking and wide application range.
WO2010132760A9 Antibacterial derivatives of tobramycin Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
CN101245059A Preparation for treating rheumatism, rheumatoid disease with caulis piperis futokadsurae amide as efficacy component The invention discloses a chemical element of a new compound caulis piperis kadsurae amide and the following chemical structure; pharmacological tests prove that the caulis piperis kadsurae amide has prominent anti-rheumatic efficacy, and a caulis piperis kadsurae capsule (containing caulis piperis kadsurae amide) which is prepared by taking the caulis piperis kadsurae amide as the efficacy ingredient obtains good effects by the trials in the clinical treatment of rheumatism.
US7538100 17α-alkyl-17β-oxy-estratrienes and intermediate products for their production, use of the 17α-alkyl-17β-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations The invention relates to 17α-alkyl-17β-oxy-estra-1,3,5(10)-trienes that have an antiestrogenic action with general formula I. In addition, the invention also relates to 17-oxo-estra-1,3,5(10)-trienes as well as 17β-hydroxy-estra-1,3,5(10)-trienes as intermediate products in the production of the estratrienes according to the invention. The invention also relates to the use of 17α-alkyl-17β-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17α-alkyl-17β-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.
US20060058273 A combination of a cephalosporin. prednisolone and a carrier to treat milk-producing animals having clinical mastis of the mammary gland; increased antiinflammatory efficiency without the immunosuppressive side effects; bovine mastitis; veterninary medicine A pharmaceutical composition for intramammary administration to a nonhuman mammal comprising an antibacterial agent and prednisolone, wherein the composition comprises at least 20 mg of prednisolone, and its use for the treatment of clinical mastitis.
CA2264582C Sulfonyl fluorides for the treatment of alzheimer's disease The present invention provides a pharmaceutical composition, comprising a sulfonyl fluoride and a pharmaceutically acceptable carrier. Also provided is a method of treating Alzheimer's disease in an individual in need of such treatment, comprising the step of administering to said individual a therapeutically effective dose of methanesulfonyl fluoride. Further provided is a method of enhancing cognitive performance in an individual in need of such treatment, comprising the step of administering to said individual a therapeutically effective dose of methanesulfonyl fluoride.
US20100098629 Novel Amides Acting on the Adenosine Receptors There are described Compounds of formula (I) in which R3 to R8 are independently selected from hydrogen, halogen, trihaloalkyl, alkyl having 1, 2, 3, 4 or 5 carbon atoms, electron donor groups selected from alkoxy having 1, 2, 3, 4 or 5 carbon atoms, trihaloalkoxy, hydroxy or amino, electron acceptor groups selected from cyano, sulphonic, nitro, or amide; R1 is an optionally substituted phenyl, benzyl or cyclohexyl group; R2 is selected from amino, substituted amino or guanidino groups, Z is a saturated or unsaturated C1-5 hydrocarbon chain, and salts thereof. A process for their preparation and compositions containing them are also described. The Compounds are either agonists or antagonists of a specific adenosine receptor or a number of adenosine receptors and have usefulness for the treatment of inflammation, arthritic conditions, rheumatoid arthritis, Osteoarthritis, mental disorders, or for inducing central nerve regeneration.
US7268149 Cyclothiocarbamate derivatives as progesterone receptor modulators and methods of treating skin disorders The present invention provides methods of treating skin disorders includes delivering to a mammal a composition containing a compound of formula I, or tautomers thereof, in a regimen, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Specifically, methods for treating acne, hirsutism, and conditioning the skin are described. Also provided are novel PR modulators of formula II.
WO2009032887A1 Methods of treating or preventing respiratory tract infection comprising administering cholecalciferol The present invention comprises an oral composition. More particularly to a method of treating and preventing a respiratory tract infection comprising: the steps of administering to a human a composition comprising from about 450 IU to about 500,000 IU of cholecalciferol, per dose of the composition.
US20060079554 Inhibitors of monomine uptake N,N-disubstituted 4-amino-piperidines of the general Formula (I) are inhibitors of the uptake of serotonin and/or norepinephrine and/or dopamine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.
CA2682613A1 Oral care compositions containing a mixed tocopherol component An oral care composition, such as a dentifrice composition, which provides enhanced anti-gingivitis efficacy is disclosed. The composition includes a tocopherol component which consists of about 10% to about 90% of gamma tocopherol, with the balance of the components selected from alpha tocopherol, beta tocopherol, delta tocopherol, and mixtures thereof.
US8415303 Method of treatment using a soluble human delta protein fragment The present invention relates to nucleotide sequences of vertebrate Delta genes, and amino acid sequences of their encoded proteins, as well as derivatives (e.g., fragments) and analogs thereof. In a specific embodiment, the vertebrate Delta protein is a human protein. The invention further relates to fragments (and derivatives and analogs thereof) of Delta which comprise one or more domains of the Delta protein, including but not limited to the intracellular domain, extracellular domain, DSL domain, domain amino-terminal to the DSL domain, transmembrane region, or one or more EGF-like repeats of a Delta protein, or any combination of the foregoing. Antibodies to Delta, its derivatives and analogs, are additionally provided. Methods of production of the Delta proteins, derivatives and analogs, e.g., by recombinant means, are also provided. Therapeutic and diagnostic methods and pharmaceutical compositions are provided. In specific examples, isolated Delta genes, from Xenopus, chick, mouse, and human, are provided.
US20120108522 Hdac inhibitors and hormone targeted drugs for the treatment of cancer The present invention relates to the methods of treating endocrine-regulated cancers, including hormone resistant cancers, for example. More specifically, the present invention relates to a method of increasing the sensitivity of hormone resistant cancers to hormonal therapeutic agents. In particular embodiments, the present invention concerns delivery of a histone deacetylase inhibitor and a hormone targeted drug to an individual with cancer. In specific embodiments, the histone deacetylase inhibitor and the hormone targeted drug act synergistically to treat the cancer, including by overcoming resistance to a cancer therapy.
CN101732451A Preparation method capable of enhancing content of amino acid of Qingkailing The invention discloses a preparation method capable of enhancing the content of the amino acid of Qingkailing, which comprises the following steps: (a) hydrolyzing buffalo horn powder; (b) hydrolyzing mother-of-pearl powder; (c) adding a right amount of concentrated H2SO4 into buffalo horn hydrolysate and mother-of-pearl hydrolysate, regulating the pH value to 3.0-5.0 and mixing; (d) concentrating the mixed supernatant liquid, chilling, adding high-concentration ethanol, refrigerating and filtering; (e) processing filtrate in the procedure of the step (d) by styrene series cation exchange resin, desorbing by using 1.0-4.0% of ammonia and collecting ammonia lotion; and (f) carrying out water bath on the ammonia lotion, drying by distillation, adding 4.0-8.0% of active carbon after adding distilled water and dissolving, and carrying out decarburization treatment. The content of various Qingkailing medicine preparations prepared by mixing a buffalo horn and mother-of-pearl mixed extract prepared by adopting the method and other medicinal materials and medicinal material extracts in a Qingkailing medicine formula and the amino acid thereof can be enhanced by 10-15%.
CN102824432A Oral liquid preparation for increasing food consumption of livestock and preparation method thereof The invention discloses an oral liquid preparation for increasing the food consumption of livestock. The oral liquid preparation comprises the following effective raw materials in parts by weight: 5-30 parts of fructus crataegi, 10-30 parts of endothelium corneum gigeriae galli, 1-2.5 parts of domperidone, 0.5-2 parts of disodium 5'-ribonucleotide, 0.2-1 part of sodium glutamate and 1-2 parts of vitamin B. A preparation method comprises the following steps of: A, weighing the effective raw materials according to the formula components; B, heating and decocting fructus crataegi and endothelium corneum gigeriae galli, concentrating, standing, cooling and filtering; and C, adding an acid cosolvent into the filtrate, sequentially adding domperidone, disodium 5'-ribonucleotide, sodium glutamate and vitamin B, and sufficiently stirring till complete solution to obtain the oral liquid preparation. In the invention, the food consumption and daily weight increase of the livestock are effectively increased through the coordination effect of the effective raw materials, and the toxic side effect and adverse reaction caused by independently using each effective raw material are reduced; and meanwhile, the preparation method provided by the invention realizes sufficient dissolution and mixing of the effective raw materials, and greatly improves the utilization rate of the effective raw materials.
CN103497860A Preparation method of buckwheat wine The invention discloses a preparation method of buckwheat wine, wherein buckwheat is abundant in nutrition, and is especially rich in active substances such as rutin and D-chiral inositol, so that the wine has a unique dietary therapy health-care effect. In common buckwheat fermented wine production process, rutin is decomposed and damaged, and the content of rutin in the buckwheat wine is very little, so that medical and edible functions of buckwheat cannot be realized, thereby, wasting the buckwheat resource. According to the invention, before fermentation of buckwheat, solvends such as food rutin are coarsely extracted, and rutin crystal mixed liquor added back after fermentation accounts for 0.1-0.5% of the wine, so that the nutritional health-care function of the wine has a synergistic effect with the rutin food. According to the technology disclosed by the invention, by means of common wine brewing equipment and process, buckwheat accounts for 3-5% of the brewing wine by just adjusting the formula, and the buckwheat rutin wine produced is slightly different from common wine in color and luster, taste, flavor and production cost. The wine contains 10-40mg/100ml of rutin, and is beneficial to patients with high blood pressure, high blood fat, cardia-cerebrovascular diseases and diabetes mellitus.
CA2635770A1 Inhibition of cxcr4 and/or cell motility by phenylalanine, cysteine or peptides containing said aminoacids The invention relates to phenylalanine, cysteine, derivatives of said amino acids, peptides comprising them, and to their use in diseases disorders or conditions whose pathology is caused by or associated with CXCR4 activity and/or cell motility.
CN1631866A Branched chain fatty acid for treating diabetes mellitus The invention relates to a compound for curing or preventing ó -type diabetes, X syndrome, adipositas and, with saturated fatty acid and unsaturated fatty acid eith sencondary and long chain on the derivative (terminal branch chain) which has general formula (I) structure, and its derivative (terminal branch chain). Its general formula is R,-CH(CnH2n-m) COOR2(I), R, is isopropyl or butyl or tertiary butyl, n is integer between 5~19 and m is integer between 0~n/2 and R2 is H or amino acid or salt of Na+, K+, Ca2+, Mg2+.
CN103070835A Freeze-dried composition containing bortezomib and preparation method of freeze-dried composition The invention belongs to the technical field of medicine, in particular to the field of chemical pharmacy, and particularly relates to a freeze-dried composition containing bortezomib and a preparation method of the freeze-dried composition. The freeze-dried composition and the preparation method aim at overcoming main medicine dissolution difficulty and oxygen environment sensitivity in an environment. A mixed solvent comprising mannitol and tert butyl alcohol is used, so that a dissolution rate of bortezomib is increased significantly, and the dissolution rate of bortezomib can be increased further through an addition sequence of materials. A nitrogen filled environment is used, so that liquid preparation time is shortened greatly, the contact of main medicine components with an aerobic environment is avoided effectively, and contents of relevant substances and total impurities in a final finished product are reduced.
CA2664572A1 Substituted piperidinophenyl oxazolidinones The present invention relates to oxazolidinones of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof. The invention also relates to processes for the preparation of the compound of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof, and to pharmaceutical compositions containing the compounds of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof and to methods for treating or preventing microbial infections using the compounds of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof.
US20120149760 Disabling autophagy as a treatment for lysosomal storage diseases Provided herein are methods of treating lysosomal storage disease, for instance Pompe disease, through inhibition of autophagy. Optionally, treatment is administered as an adjunct to enzyme replacement therapy (ERT).
CN101816674A Hepcidin inhibitor and application thereof The invention provides a hepcidin inhibitor. The hepcidin inhibitor is angelica polysaccharides. The angelica polysaccharides hepcidin inhibitor provided by the invention can inhibit the expression of hepcidin of normal rats and iron-deficiency anemia rats so as to increase the absorption of small intestines on iron and the release of a reticuloendothelial system on iron and improve iron-deficiency symptoms of the body. The hepcidin inhibitor of the invention is a natural product. A preparation process for the hepcidin inhibitor has the advantages of simple preparation, high yield, little pollution, low cost and no toxic or side effect, and is suitable for preparing a medicament for treating diseases caused by hepcidin over-expression.
US7259152 Oral administration of Sulodexide in unit dosages suitable for the treatment of diabetic nephropathies in both macro and micro albuminic patients, producing immediate and lasting improvement in albumin excretion rate The present invention provides oral formulations of Sulodexide for the treatment of diabetic nephropathy in patients with both insulin dependent and non-insulin dependent diabetes mellitus. Oral formulations containing doses adapted for administration to obtain a reduction in albumin excretion in patients with both micro and macro albuminuria and to produce lasting improvement in albumin excretion rate are provided. Methods of treating diabetic nephropathy using these formulations are also provided.
CN102321625A Small molecular double stranded RNA group prepared from yeast, preparation method and use thereof The present invention discloses a small molecular double stranded RNA group prepared from yeast, a preparation method and a use thereof. According to the present invention, the small molecular double stranded RNA group is prepared through adopting a mixture and the total RNA of the yeast as substrates, wherein the mixture comprises at least two selected from ribonuclease T1, deoxyribonuclease I and ribonuclease III, the yeast is the yeast which kills plasmids. The small molecular double stranded RNA group provided by the present invention can be provided for preparing cancer prevention care products, anti-cancer health care products and anti-virus health care products. The preparation method provided by the present invention is simple, and is easy to operate.
EP1347751B1 Methods of treating bone cancer and the pain associated therewith using endothelin antagonists The instant invention is directed to methods for the inhibition of bone metastases, methods for the prevention of growth of new metastases, methods for the inhibition of bone turnover, and methods for the prevention of bone loss in patients, including cancer patients, using an endothelin ET-A receptor antagonist.
EP1518854A1 Substituted 06- benzylguanines and 7- or 9- substituted 8-aza-06-benzylguanines The present invention provides AGT inactivating compounds such as 7- or 9-substituted 8- aza- O6-benzylguanines of formula (III) or (IV), and related substituted O6-benzyl guanines, as well as pharmaceutical compositions comprising such compounds along with a pharmaceutically acceptable carrier. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumour cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesions at the O6- position of guanine, by administering to a mammal an effective amount of one of the aforesaid compounds, 2,4-diamino-6-benzyloxy-s-triazine, or 8-aza-O6-benzylguanine, and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O6- position of guanine.
CN103393682A Compound medicinal composition of felodipine The invention relates to a use of the combination of felodipine and pitavastatin calcium in the treatment of hyperlipidemia and hypertension, a compound medicinal composition containing felodipine and pitavastatin calcium, a compound medicinal composition containing slow-release felodipine and quick-release pitavastatin calcium, and a treatment method for the hypertension with hyperlipidemia through the combination.
CN102349871A Nano-micro drug delivery system and preparation method of 10-hydroxyl camptothecin The invention relates to a nano-micro drug delivery system and a preparation method of a slightly soluble drug of 10-hydroxyl camptothecin (HCPT). The invention makes use of alginate to dissolve HCPT under alkalic condition; then acidic calcium chloride miniemulsion is added to the prepared uniform HCPT-containing emulsion to have crosslinking and curing reactions; at the time when the emulation droplets cure, the HCPT constellation is partially transformed, so that the HCPT crystallize; and then, an acidic chitosan solution or an acidic chitosan derivative is used for secondly curing so as to let the HCPT to crystallize further more. The product prepared through the method is a composite alginate chitosan microsphere or a micro-capsule drug delivery system loaded with HCPT with uniform size and stable dispersion. The nano microspheres of the system have uniform grain size and stable dispersion and the drugs in the nano microspheres exist in the form of closed-loop medicinal nanocrystalline. The invention can realize the increase of solubility of indissolvable drugs and the improvement of bioavailability and effectively improves the encapsulation rate of the indissolvable drugs.
US20110009416 PH INDEPENDENT FORMULATIONS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-OXO-6,7-DIHYDRO-5H-PYRROLO[3,4-b]PYRAZINE Pharmaceutical compositions of zopiclone [(6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine)] that render the aqueous solubility/dissolution of the free base independent of the pH of the gastrointestinal tract are disclosed. The compositions are useful for oral administration.
US20080249118 diagnosing prostate carcinoma by determining the methylation degree in the genomic locus of a gene selected from the group consisting of 14-3-3 sigma , DDB2, GPX3, GSTM1, SFRP1, DKK3, p57/KIP2, COX-21PTGS2, HPGD and combinations thereof in a sample, wherein a hypermethylation is indicative of cancer The present invention relates to method and kits for diagnosing and/or treating prostate cancer. The method and kit relate to the determination and/or modulation of the methylation degree of tumor suppressive genes in biological samples. More particularly, CpG-methylation of 14-3-3σ was found in all primary PCa samples analysed, but not in matching normal prostate epithelial cells or benign prostate hyperplasia (BPH). CpG-methylation was accompanied by a decrease or loss of 14-3-3σ protein expression in primary PCa and PCa cell lines. PCa-precursor lesions, known as prostatic intraepithelial neoplasia (PIN), also displayed decreased levels of 14-3-3σ expression, whereas normal prostate epithelial cells and BPH showed high levels of 14-3-3σ protein expression. The generality of CpG-methylation in PCa suggests that silencing of 14-3-3σ significantly contributes to the formation of PCa. Furthermore, the CpG-methylation of 14-3-3σ in PCa may be exploited for diagnostic purposes.
WO2011136159A1 Composition for the treatment of aesthenopia Disclosed are a novel drug and a food or drink composition for the treatment of aesthenopia which are effective in ameliorating aesthenopia. The disclosed composition for the treatment of aesthenopia is formed by a mixture with condroitin sulfate or a salt thereof.
WO2009006839A1 Substituted indol-3-yl oxalylpodophyllotoxin derivates, their salts, and application thereof Substituted indol-3-yl oxalylpodophyllotoxin derivates and their salts comprise the following general formula (I). These compounds are effective against many drug-resistant tumors.
CN103202813A Method for preparing protein nanoparticles for in vivo delivery of pharmacologically active substances The present invention relates to a method for preparing protein nanoparticles for in vivo delivery of pharmacologically active substances, which belongs to the field of in vivo delivery of pharmacologically active substances and clinical applications thereof. The invention adopts the method of expanding and then refolding, or self-assembly of proteins and peptides for pharmacologically active substances to be included into protein nanoparticles for in vivo delivery.
CN103622914A [4-(2-methylphenylsulfonyloxy)-2(3H)-benzoxazolone] liposome The invention relates to the field of medicine, in particular to a [4-(2-methylphenylsulfonyloxy)-2(3H)-benzoxazolone, MBB] liposome. The liposome is prepared by the following raw materials by weight percentage: 0.5-2.5% of [4-(2-methylphenylsulfonyloxy)-2(3H)-benzoxazolone], 6-12% of phospholipid, 0.8-1.4% of cholesterol, 1.1-2.3% of tween-80, 0.5-1.5% of antioxidant, and the balance of buffer solution with concentration of 0.05mol/L and pH (power of hydrogen) of 6-8, wherein the buffer solution is selected from a phosphate buffer solution, a citrate buffer solution and a carbonate buffer solution. An encapsulation rate of the MBB liposome is at least above 90%; the characteristic of a liposome entrapment drug is met; the change of the encapsulation rate of the liposome during the storage period is not obvious; compared with an MBB compound, the degradation of the liposome is reduced obviously, and the stability is improved; and the liposome has an exact therapeutic effect on arthritis.
CN102988323A Preparation method of aniracetam sustained-release tablet The invention relates to an aniracetam sustained-release tablet for treating senile dementia, belonging to the technical field of Western medicine preparation. The aniracetam sustained-release tablet is formed by a base tablet and a coating, and is characterized in that according to total weight percentage of the sustained-release tablet, the base tablet is formed by the following components: 30-70 parts of aniracetam, 10-30 parts of carrageenan, 1-10 parts of lubricating flow aid, 5-15 parts of citric acid and 1-20 parts of sweetening agent; and the coating is formed by the following components: 0.5-3 parts of sodium carboxymethylcellulose, 0.5-5 parts of propylene glycol and 0.5-2 parts of lubricating flow aid based on the total weight of the sustained-release tablet being 100 parts. The tablet disclosed by the invention is sustained in release, has weak side effect on the stomach and intestine, and does not have bitter taste.
WO2013009586A1 Topical minocycline ointment for suppression of allergic skin responses The method of the present application is directed towards a method for suppressing an allergic response in response to an allergic trigger. This method comprises the following steps; applying, topically, to an affected area an effective amount of a minocycline composition so that the minocycline composition contacts the affected area for an effective amount of time and removing the minocycline composition from the affected area.
WO2005025574A2 PTERIDINE DERIVATIVES FOR THE TREATMENT OF SEPTIC SHOCK AND TNF-α-RELATED DISEASES. This invention relates to the use of a group of pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, for the manufacture of a medicament for the prevention or treatment of TNF-α related disorders.
US20130039847 Liposomes for pulmonary administration The invention relates to liposomes for pulmonary application, advantageously comprising at least one first and at least one second phospholipid, cholesterol, and at least one active substance and/or colorant, wherein the first phospholipid is a phosphatidylcholine, preferably DSPC, and the second phospholipid is a phosphatidylcholine or an ethanolamine, preferably selected from the group DMPC, DPPC, DPPE. It is thereby advantageous if the first and the second phospholipid are present at a molar ratio of 0.5:1 to 10:1, preferably at a ratio of 6:1 to 2:1, in particular preferably at a ratio of 3:1. It is further advantageous if the molar ratio between phospholipids and cholesterol is between 10:1 and 1:1, preferably between 6:1 and 3:1, in particular preferably 4:1. The second phospholipid is further preferably DMPC or DPPE, in particular preferably DPPE. The size of the liposomes is advantageously between 0.05 μm and 5 μm, preferably between 0.2 μm and 2.0 μm, and the median aerodynamic mass diameter of aerosol particles comprising the liposomes is between 1 μm and 6 μm, preferably between 1.5 μm and 5 μm, in particular preferably between 2 μm and 4.5 μm. It is further in particular advantageous if the liposomes comprise an atomization stability of greater than 50%, preferably greater than 75%, in particular preferably greater than 80%, and if the transition temperature is greater than 37° C., preferably greater than 45° C., in particular preferably greater than 50° C.
CN102697764A Enteric solid preparation containing phenethyl isothiocyanate The invention relates to an enteric solid preparation containing an active ingredient phenethyl isothiocyanate. The enteric solid preparation comprises an enteric polymer material and the phenethyl isothiocyanate. The CAS number of the phenethyl isothiocyanate is 2257-09-2, and the weight of the phenethyl isothiocyanate occupies 5%-65% of total weight of the enteric solid preparation. The enteric solid preparation can lighten stimulation to gastric mucosa and can be prepared into a stable pharmaceutical preparation, the volatility is overcome, and the clinical compliance can be improved.
CN103387549A Racemates and optic isomers of three benzotriazolarylpiperazine compounds, and preparation method and use of racemates and optic isomers The invention relates to racemates of three benzotriazolarylpiperazine compounds 1-(1-benzotriazoloxy)-3-(4-(2-methoxyphenyl or ethoxyphenyl or chlorophenyl)piperazine)-2-propanol, optic isomers of the three compounds, and a preparation method and a use of the racemates and the optic isomers. The preparation method comprises the following steps: reacting 1-hydroxybenzotriazol with chloropropylene oxide to obtain a racemate of an epoxy intermediate, or reacting 1-hydroxybenzotriazol with R-glycidyl tosylate or S-glycidyl tosylate to obtain an R-optic isomer or an S-optic isomer of the epoxy intermediate; and respectively reacting the racemate of the epoxy intermediate, or the R-optic isomer or the S-optic isomer of the epoxy intermediate with o-methoxyphenylpiperazine, o-ethoxyphenylpiperazine or o-chlorophenylpiperazine to obtain above products. Experiments prove that the prostatoplasia resistance activities of seven compounds in the above nine compounds are stronger than that of a contrast drug prazosin.
EP1833487A1 New use of gabab receptor agonists The present invention relates to the use of phosphinic acid derivatives according to formula (I) and (II) as well as sulfinic acid derivatives according to formula (III) for the treatment or prevention of cough.
CA2364944C C16 unsaturated fp-selective prostaglandins analogs The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, X, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of said formula, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders using these compounds or the compositions containing them.
CA2731769C Controlled-release otic structure modulating and innate immune system modulating compositions and methods for the treatment of otic disorders Disclosed herein are compositions and methods for the treatment of otic disorders with otic structure modulating compositions administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and compositions onto or via perfusion into the targeted auris structure(s).
WO2006082129A1 Use of tyrosine kinase inhibitors for the treatment of chronic rhinosinusitis The invention relates to the use of selected EGFR kinase inhibitors, especially selected quinazolines, quinolines, and pyrimidopyrimidines, for treating nasal polyposis and chronic rhinosinusitis.
DE102009015070A1 New phenyl-pyrimidin-2-yl-amine compounds are tyrosine kinase 2 inhibitors useful for treating e.g. rheumatoid arthritis, Crohn's disease, asthma, multiple sclerosis, adult respiratory distress syndrome, allergic alveolitis and uveitis Phenyl-pyrimidin-2-yl-amine compounds (I) and their salts, diastereomers or enantiomers are new. Phenyl-pyrimidin-2-yl-amine compounds of formula (I) and their salts, diastereomers or enantiomers are new. Either R1a, R1b : 1-6C-alkyl, 2-6C-alkenyl, 3-6C-cycloalkyl, a monocyclic or bicyclic heteroaryl, or phenyl group (all optionally substituted by halo, OH, 1-6C-alkyl or 1-6C-alkoxy), H, heterocycloalkyl with 3-6 ring atoms, or a monocyclic heteroaryl or bicycle; or R1aR2aN : a heterocycloalkyl with 3-6 ring atoms (optionally additionally containing 1 or 2 further heteroatoms, optionally interrupted by one or more CO, optionally containing double bonds and/or optionally substituted by OH, halo, 1-6C-alkyl, NR1aR1b or NHCOR 8>); R 8>1-6C-alkyl, 2-6C-alkenyl, 3-6C-cycloalkyl, a heterocycloalkyl with 3-6 ring atoms, a monocyclic or bicyclic heteroaryl or phenyl (optionally substituted by halo, OH, 1-6C-alkyl, 1-6C-alkoxy, 1-6C-alkylthio, 3-6C-cycloalkyl, heterocycloalkyl with 3-6 ring atoms, a monocyclic or bicyclic heteroatoms, or phenyl); R 2>2-6C-alkyl substituted by OH; R 3>H or F; R 4>, R 5>H, halo, CH 3or CF 3; and R 6>H or halo. An independent claim is included for the preparation of (I). [Image] - ACTIVITY : Antiarthritic; Antirheumatic; Antiinflammatory; Gastrointestinal-Gen.; Antiasthmatic; Neuroprotective; Respiratory-Gen.; Dermatological; Muscular-Gen.; Immunosuppressive; Vasotropic; Antipsoriatic; Nephrotropic; Hepatotropic; Virucide; Antiulcer; Ophthalmological; Cytostatic; Hemostatic; Antidiabetic; Gynecological. - MECHANISM OF ACTION : Tyrosine kinase 2 inhibitor. The ability of (I) to inhibit tyrosine kinase 2 was tested in Baculovirus infected insect cells using tyrosine kinase 2 homogeneous time resolved fluorescence. The results showed that morpholin-4-carboxylic acid-{3-(4-[(S)-1-hydroxymethyl-et hylamino)-pyrimidin-2-ylamino]-phenyl}-amide exhibited an IC 5 0value of 1.01E-07 mol/l.
US20100292169 Methods and compositions for regulating hdac6 activity The present invention provides methods and compositions for inhibiting Hsp90 activity in a cell, comprising contacting the cell with an inhibitor of histone deacetylase 6 (HDAC6)
US20090136588 Methods For Altering Food Intake, Modifying Nutrient Digestibility and Altering Stool Quality and/or Stool Frequency The invention encompasses methods for altering food intake, modifying nutrient digestibility and altering stool quality and/or stool frequency in an animal by adjusting the balance of metabolizable cations to metabolizable anions consumed by the animal.
WO2007031879A3 Lipid a analogs for treating oral and gastrointestinal mucositis The invention provides methods of reducing the severity of oral and gastrointestinal mucositis, involving administration of a toll-like receptor 4 antagonist.
WO2010010138A1 Pharmaceutical composition comprising pramipexole and a calcium channel blocker for the treatment of parkinson's disease The invention relates to a new medication for the treatment of the cardinal symptoms of Parkinson's disease. The medication comprises the administration of pramipexole or a pharmaceutically acceptable salt thereof and a calcium channel blocker or a pharmaceutically acceptable salt thereof. The medication is a combination of pramipexole or a pharmaceutically acceptable salt thereof and said calcium channel blocker or a pharmaceutically acceptable salt thereof which may be used in a fixed-dose combination as well as in a free-dose combination.
US20100172860 Wound repair composition and method The invention provides a dressing composition comprising a bisphosphonate matrix metalloproteinase (MMP) inhibitor covalently bound to a polymer wherein, when the dressing is contacted with a wound, substantially all of the bisphosphonate remains with the dressing composition and is unable to enter the wound tissue. The invention also provides for a method of treatment of a wound by contacting a dressing composition comprising a covalently bound MMP inhibitor with the wound fluid to thereby selectively inhibit one or more MMP's in the wound fluid without inhibiting those in the wound tissue.
WO2006030984A1 Piperidine compound and process for preparing the same The present invention is to provide a piperidine compound represented by the formula [I]: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted benzene ring, R1 is hydrogen atom or a substituent for amino group, R2 is hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom, Z is oxygen atom or -N(R3)-, R3 is hydrogen atom or an optionally substituted alkyl group, R4a and R4b may be the same or different, and each is hydrogen atom or an optionally substituted alkyl group, or a pharmaceutically acceptable salt thereof, which has an excellent tachykinin receptor antagonistic action.
EP2451451A1 Hdac 6 inhibitor-based methods for treating cancer This invention provides methods for treating a subject afflicted with cancer, comprising concurrently administering (i) an HDAC 6-selective inhibitor and (ii) a suitable cytotoxic agent such as SAHA, doxorubicin or etoposide. This invention also provides methods for inducing the death of a transformed cell such as a cancer cell, comprising concurrently contacting the cell with (i) an HDAC 6-selective inhibitor and (ii) a suitable cytotoxic agent such as SAHA, doxorubicin or etoposide.
WO2012061907A3 Osteoclast activity The invention relates to medicaments and novel methods of treating metabolic bone diseases, and more particularly for treating or preventing Critical Illness Related Metabolic Bone Disease or of critical illness induced Osteopenia [ICD-10 M85.8, ICD-9 733.90, DiseasesDB 29870 or MeSH D001851] secondary to ICU Admission by sufficient autophagy inducing compound to inhibit or suppressing critical illness [MeSH Descriptor: C23.550.291.625] enhanced osteoclastogenesis or increased osteoclast differentiation. The disclosed therapeutic methods include administering of a autophagy activating compound to a mammal to: (1) treat or prevent a bone degenerative disorder; (2) slow bone deterioration; (3) restore lost bone; (4) maintain bone mass and/or bone quality or (5) inhibit bone resorption in particularly by inhibiting or reducing a process by which osteoclasts break down bone and release the minerals resulting in a transfer of calcium from bone fluid to the blood. The invention also provides methods for administering the autophagy activating compound to treat a bone disorder of hyperresorption of bone and/or enhanced activation of osteoclasts.
US20060052389 Compositions and methods for enhancing analgesic potency of tramadol and attenuating its adverse side effects The invention generally relates to compositions and methods with tramadol and an opioid antagonist to enhance analgesic potency and/or attenuate one or more adverse effects of tramadol, including adverse side effect(s) in humans such as nausea, vomiting, dizziness, headache, sedation (somnolence) or pruritis. This invention relates to compositions and methods for selectively enhancing the analgesic potency of tramadol and simultaneously attenuating anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects associated with the administration of tramadol. The methods of the present invention comprise administering to a subject an analgesic or subanalgesic amount of tramadol and an amount of excitatory opioid receptor antagonist such as naltrexone or nalmefene effective to enhance the analgesic potency of tramadol and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of tramadol.
CN103520144A Application of dianhydrogalactitol in preparation of medicines for treating cervical cancer The invention relates to the research on the influence of dianhydrogalactitol on HeLa cell proliferation and cell cycle control. After HeLa cells are treated by dianhydrogalactitol with different concentrations for 24 hours, cell cycle analysis results prove that the content of the cells in a G1 phase is obviously higher than that of a control group (P is less than 0.01); Western blot results prove that dianhydrogalactitol can be used for reducing the expression of HeLa cyclin D1; meanwhile, ELISA (Enzyme Linked Immunosorbent Assay) results also prove that dianhydrogalactitol can be used for down-regulating the expression of CDK4 and enhancing the expression of a CDK inhibitor P21; RT-PCR (Reverse Transcription-Polymerase Chain Reaction) experimental results also prove that dianhydrogalactitol can be used for reducing the mRNA (Message RNA) level of the cyclin D1, CDK2 and CDK4 in the HeLa cells and up-regulating the expression of P21 on the mRNA level. Therefore, dianhydrogalactitol can be used for blocking the HeLa cells in the G1 phase, thus the proliferation of the cells is restrained.
WO2009084739A1 Method and pharmaceutical composition for treatment of cancer using bmp10 protein, Disclosed is a therapeutic agent for cancer, which can treat solid cancer or a disease or disorder associated with the solid cancer without inducing any adverse side effect. Specifically disclosed is a pharmaceutical composition for treating and/or preventing cancer, which comprises BMP10 protein, a nucleic acid encoding BMP10 protein, an expression vector carrying a nucleic acid encoding BMP10 protein, or a combination of two or more of them as an active ingredient.
EP1075186B1 Method of hsv prophylaxis Herpes virus infection can be prevented by the topical application of metallo-organic cobalt compounds according to formula (I) to the site of infection, wherein each A may be the same or different and is an alkyl group, a phenyl group or a substituted derivative of a phenyl group; wherein each Y may be the same or different and is hydrogen, an unbranched alkyl group, a halide or a group having the structure of formula (a) wherein R is hydrogen, an alkoxide group, and alkyl group, or OH; wherein each B may be the same or different and each is hydrogen or an alkyl group; wherein each X may be the same or different and each is a water soluble group having weak to intermediate ligand filed strength; and Z- is a soluble, pharmaceutically acceptable negative ion. Metallo-organic cobalt compounds may also be used to disinfect liquids which contain herpes virus.
US20120288551 Implantable Polymeric Device for Sustained Release of Sufentanil Extended release of sufentanil is provided by implanting a device containing sufentanil into a mammal or human being. The device may include a solid biocompatible polymer matrix, and sufentanil may be encapsulated within the polymer matrix. The polymer matrix comprises a plurality of pores configured to allow contact between the sufentanil and a physiological fluid of a mammal into which the device is implanted to thereby release sufentanil in vivo from the device into the mammal. The devices may be used to treat opioid addiction or pain.
CN102908328A Fudosteine composition tablet and preparation method thereof The invention relates to the field of pharmaceutical preparation, and in particular relates to a fudosteine composition tablet and a preparation method of the fudosteine composition tablet. The invention provides the fudosteine composition tablet and the preparation method of the fudosteine composition tablet. The fudosteine composition tablet is good in stability; and when the method is adopted for tabletting, the tablet is not easily broken, so that the operation steps are simplified, and industrial production can be easily realized.
US20110009476 Transcription factor decoys, compositions and methods Compositions and methods for identifying and using cis-regulatory and decoy sequences.
CN101822640A Sulbenicillin sodium liposome injection The invention discloses a sulbenicillin sodium liposome injection, which is characterized by comprising the following components in part by weight preferably: 1 part of sulbenicillin sodium, 3 to 5 parts of soya bean lecithin, 0.8 to 2 parts of cholesterol, 0.2 to 1 part of dipalmitoyl phosphatidylethanolamine, 0.1 to 0.5 part of antioxygen and 5 to 10 parts of excipient. The liposome injection prepared by the invention has the advantages of obvious technical effect, high dissolvability and stability, high encapsulating rates, small side effect, high bioavailability and obvious curative effect.
US7011851 Drug delivery; incontinence therapy Disclosed are oxidized collagen compositions wherein the thiomethyl group of one or more of the methionine residues of the collagen have been replaced with methylsulfoxy and/or methylsulfonyl groups.
US20110105433 Lecithin and lc-pufa The present invention relates generally to the prevention/and or stopping of the generation of off-flavours in food products. In particular is the present invention directed to the formulation of lipid raw material mixes and food products containing long chain polyunsaturated fatty acids, and to compositions and processes for stabilizing such products against the formation of off-flavours, such as fishy off-odours. One embodiment of the present invention is a composition comprising an LC-PUFA containing oil and lecithin, wherein weight ratio of lecithin to LC-PUFA is at least about 25:75.
US20090087407 Methods for the treatment of scleroderma using 1-oxo-2-(2,6-dioxopiperidin-3-yl)-4-methylisoindoline Methods of treating, preventing, correcting and/or managing skin diseases or disorders characterized by overgrowths of the epidermis, keratoses, scleroderma, cutaneous vasculitis, acne or wrinkles are disclosed. Specific embodiments encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent. Specific second active ingredients are capable of affecting or inhibiting cell growth or proliferation, removing or improving acne scars, or reducing or correcting wrinkle lines. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
EP1551440A2 Uses of human zven proteins and polynucleotides The present invention provides methods of using Zven1 and Zven2 polypeptides to increase chemokine production. The present invention also provides methods for treating intestinal motility disorders and improving gastrointestinal funciton with Zven1 and Zven2 polypeptides.
US20120189682 Inhibition of biofilm organisms The present invention relates to a product comprising at least two antibiofilm agents wherein at least one of the antibiofilm agents is an antimicrobial peptide. The second antibiofilm agent is generally a dispersant or an anti-adhesive agent. There is also provided the use of the product in the treatment of a microbial infection.
CA2658223A1 Benzopyranopyrazoles Compounds of a certain formula (I), in which Ra, Rb and Rc have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.
US20080167361 Piperazinyl-substituted quinolinone compounds ;to treat nervous system diseases, neurodegenerative diseases; gastrointestinal tract disorders; cognition enhancers; 3-[4-(3-Ethylsulfanyl-benzenesulfonyl)-2-methoxy-phenyl]-pyrrolidine and 5-(3-Ethylsulfanyl-benzenesulfonyl)-2-pyrrolidin-3-yl-phenol Compounds of the formula I: wherein m, n, Ar, R1 and R2 are as defined herein. Methods of making the compounds and using the compounds are disclosed.
US20080280848 Structures of Active Guide Rna Molecules and Method of Selection The present invention relates to methods and compositions for modulating RNA silencing efficiency by providing selective RISC (RNA-induced silencing complex) formation. The present invention also relates to methods for identifying nucleic acids and/or determining their structures.
US20100197724 6.5 -pyrrolopiperidine tachykinin receptor antagonists The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.
US20080160088 Used for preventing and/or reducing the embrittlement of the skin and/or semi-mucous membranes and/or for protecting the skin and/or semi-mucous membranes against water loss and/or external attack; comprises calcium salt preferably calcium pantetheine sulfonate Composition containing, preferably in a physiologically acceptable medium, at least hydroxyapatite that is at least partially in free form and at least one calcium salt. Method of use. The invention method and composition is preferably used for preventing and/or reducing the embrittlement of the skin and/or semi-mucous membranes and/or for protecting the skin and/or semi-mucous membranes against water loss and/or external attack
CN101160291B Novel hsp90 inhibitor Disclosed is a triazole derivative represented by the general formula (1) below or a pharmacologically acceptable salt thereof. Also disclosed are a prodrug of such a triazole derivative and an HSP90 inhibitor containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or amino group or the like.
WO2012117396A1 Tyrphostin derivative in combination with cytotoxic compounds for treating cancer The present invention relates to compositions and methods for treating cancer, by administering a combination comprising a tyrphostin derivative and at least one other anti-cancer agent. The tyrphostin derivative and the at least one other anti-cancer agent together provide a therapeutic anti-cancer effect, which is additive or synergistic.
CA2657821A1 Aza-peptide protease inhibitors The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and /or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
US20050154048 cysteine proteases, cathepsin K; bone metabolic enzymes inhibitor; bone resorption process; anticarcinogenic; 5-[1-(hydroxyimino)ethyl]-2-thiophenecarboxylic acid 2-[[(9H-fluoren-9-yl)methoxy]carbonyl]hydrazide; esterification and coupling with diamine compounds of thiophenecarboxylic acid derivatives The invention concerns novel compounds of formula (I), process for making, pharmaceutical compositions and methods of treating diseases associated with abnormal physiological behavior in the secretion and/or the activity of cysteine proteases especially cathepsins.
US20080131483 Enhancement of Drug Delivery to the Central Nervous System A method for targeting the central nervous system, for use in the treatment and/or prevention of central nervous system disorders and/or states, comprising administering to a subject in need of treatment an effective amount of a pharmaceutical composition by the ocular route of drug delivery.
US20080085311 Antihistamine-decongestant combinations Multi-particulate pharmaceutical compositions comprising an antihistamine for immediate release and a decongestant for modified release.
US8367656 Polymorphs of 7-[(3-chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid S,S-dioxide used to treat depressive disorders, irritable bowel syndrome, attention deficit hyperactivity disorder, asthma Disclosed herein are novel polymorphs of 7-[(3-chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid S,S-dioxide. Also described herein are novel pharmaceutical compositions comprising one or more 7-[(3-chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid S,S-dioxide polymorphs, methods of making, and related methods of treatment.
US20110195961 Tricyclic oxazolidinone antibiotic compounds The invention relates to antibacterial compounds of formula I wherein is a bond or is absent, V is CH, CR6 or N; R0 is H or, if is a bond, may also be alkoxy; R1 is notably H or halogen; U is CH or N when is a bond, or, if is absent, U is CH2, NH or NR9; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.
EP2218450A1 Memantine for treating bipolar mood disorders resistant to conventional treatments The present invention refers to the use of Memantine for the preparation of an antimanic and mood stabilizer medication to treat treatment-resistant bipolar mood disorders. In particular, for the prevention of the switch from depression to mania/hypomania, spontaneous or induced by antidepressant treatments, for the therapy of mania and prophylaxis of type I and II bipolar disorders resistant to currently used treatments, for the therapy and prophylaxis of rapid-cycling bipolar disorder resistant to treatments currently in use, for the therapy and prophylaxis of mixed bipolar episodes resistant to treatments currently in use and for the therapy and prophylaxis of bipolar disorder with psychotic symptoms resistant to standard treatments. The use described in the present invention is absolutely at variance with prevalent hypotheses which take Memantine to be a potentially antidepressant drugs.
US20100041649 viricides used for for treating a human papillomavirus (HPV) viral infections, for inhibiting HPV DNA replication or for preventing prenatal transmission of HPV from mother to baby by administering to the mother prior to giving birth A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A, X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.
US20110097334 Novel Marker Genes for Regulatory T Cells from Human Blood The present invention provides novel marker genes for the specific identification and characterization of human suppressive and/or regulatory T cells including natural, adaptive, and expanded CD4+CD25+FOXP3+ T cells in healthy individuals as well as tumor patients or patients with autoimmune diseases.
CN101177421B Method for preparing high-purity taxone compounds The invention discloses a method for preparing taxol, docetaxel and other taxanes. The taxanes synthesized or semi-synthesized or extracted from the plants are used as the raw materials, the waterborne solvent is used to dissolve the materials, and the macroporous absorption resins such as Diaion Hp resins, Amberlite XAD resins are used as the stationery phase, the organic solvents such as THF, N, N-DMF and other solvents are used as the eluent, the atmospheric pressure column chromatography is adopted, one step is enough to extract the taxanes with the purity above 99.90% with high yield above 99.0%. The invention has the advantages of simple method, convenient operation, favorableness to production expansion, small amount and recyclability of organic solvent and environmental friendliness.
EP1567526B1 Carbamic acid esters with anticholinergic action The invention relates to novel carbamic acid esters of general formula (1), in which X- and the groups A, R1, R2, R3 and R4 can be defined as cited in the claims and the description. The invention also relates to a method for producing said esters and to their use as medicaments, in particular medicaments with an anticholinergic action.
WO2006079644A1 Indolopyridines, benzofuranopyridines and benzothienopyridines Compounds of a certain formula (I), in which R1 , R2, R3, R4, R5 and X have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity.
CN103251572A Preparation method of theaflavin enteric microcapsule, as well as product prepared by preparation method and application of product The invention discloses a theaflavin enteric microcapsule particle, a preparation method and an application thereof. The preparation method comprises the following steps of: (1) dissolving 2-8 parts by weight of a capsule material, which is an enteric material, into a 80%-95% ethanol water solution to prepare 1%-8% capsule material solution, dissolving 0.5-2 parts by weight of theaflavin-containing tea extract into distilled water to obtain 0.15%-2% core material solution, adding 2%-5% of stearic acid into the core material solution, and stirring and emulsifying to obtain a core material emulsion; and (2) mixing the capsule material solution and the core material emulsion, uniformly stirring, adding 0.01-0.1 part by weight of an antisticking agent and 1-8 parts by weight of castor oil and/or span-80 into a mixture, stirring and emulsifying to obtain an emulsion, and drying the emulsion, wherein the weight ratio of the core material to the capsule material is 1:2 to 1:8. A theaflavin enteric microcapsule disclosed by the invention is simple in preparation method and process, good in stability, convenient to store and transport, uniform in granularity, good in dispersibility, high in medicament encapsulation rate and dissolubility and capable of being widely applied to the fields, such as health-care products, medicaments and the like.
CN103054891A Compound erythromycin thiocyanate composition for controlling poultry bacterial and mycoplasma infection and preparation method thereof The invention relates to a compound erythromycin thiocyanate composition for controlling poultry bacterial and mycoplasma infection and a preparation method thereof. The composition is prepared by uniformly mixing the following components according to parts by weight: 10-15 parts of erythromycin thiocyanate, 10-20 parts of neomycinsulphate, 4-7 parts of trimethoprim lactate and 58-76 parts of anhydrous dextrose. The compound erythromycin thiocyanate composition for controlling poultry bacterial and mycoplasma infection has the beneficial effects of being reasonable in composition, simple for preparation and very obvious in curative effect, and has specially good effect for curing poultry bacterial and mycoplasma infection through clinical application.
CN101549102A A bone fracture setting ointment and method for preparing same The invention discloses a bone fracture setting ointment and method for preparing same. The bone fracture setting ointment is prepared by the following components: standard roots, Eupolyphaga, keel, crabs, wild grape root, Wu Chia Pee, alpine yallow herb, kusnezoff monkshood, Sichuan aconite root, strychnos nux-vomica, datura flower, pyrite, cassia twig, Asarum, monkshood, Eupatorium japonicum, borneol, gentiana macrophylla pall, notoginseng, buck grass, bark of eucommia, black bone, Drynaria, angelica, frankincense, myrrh, bletilla, aucklandia root, loranthus mulberry mistletoe, amber, elder, Vaseline, sesame oil, and wine. The method includes: placing the Vaseline into the wok, simmering, removing the fire and adding in benne oil and wine, and then adding the other components in the wok, stirring evenly and then spreading cool to form the bone fracture setting ointment. The invention can rapidly disperse the swelling and stop the pain, quicken the bone healing without any stimulation to the skin and any toxic side effects.
US7220771 Jun n-terminal kinase inhibitors Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
CN102727463A Formula and preparation method for ursodeoxycholic acid soft capsules The present invention relates to a formula and a preparation method for ursodeoxycholic acid soft capsules. The formula comprises ursodeoxycholic acid, a vegetable oil, paraffin wax and lecithin. The present invention further discloses the preparation method for the ursodeoxycholic acid soft capsules, wherein the method has characteristics of simple operation and low cost. With the ursodeoxycholic acid soft capsules prepared by the method of the present invention, effects on liver protection and bile flow prompting by the ursodeoxycholic acid can be significantly improved. The product of the present invention can be applicable for treatments of fatty liver, cirrhosis, gallstones, and other liver and gallbladder diseases.
EP1671644A2 Pharmaceutical compositions containing Lysostaphin alone or in combination with an antibiiotic for the treatment of Staphylococcal infections Lysostaphin is demonstrated to be a powerful ani-staphylococcal agent suitable for parental administration to mammals including humans. Low dosages, on the order of 0.5 - 45 mg/kg/day are sufficient to eradicate most staphylococcal infections. Lysostaphin is also effective against bacteria of this type which have developed resistance to conventional antibiotics such as penicillins and vancomycin. Lysostaphin analogues, such as variants and related enzymes, show similar activity.
US20090074862 Low-dose doxepin formulations and methods of making and using the same The invention disclosed herein generally relates to low-dose oral doxepin pharmaceutical formulations and the use of these formulations to promote sleep.
WO2009038110A1 Agent having neurotrophic factor-like activity Disclosed is a pharmaceutical agent having high safety and a neurotrophic factor-like activity, which comprises, as an active ingredient, any one compound included in fatty acids each having 8 carbon atoms (C8) or having 10 carbon atoms (C10) to 12 carbon atoms (C12) or esters of the fatty acids, such as ethyl 3,7-dimethyloctanoate ester, ethyl geranate ester and the like each of which has 8 carbon atoms (C8), methyl decanoate ester, trans-2-decenoic acid, methyl trans-2-decenoate ester, ethyl trans-2-decenoate ester, 2-decenyl trans-2-decenoate ester, cyclohexyl trans-2-decenoate ester, isopropyl trans-2-decenoate ester, methyl trans-3-decenoate ester, methyl trans-9-decenoate ester and the like each of which has 10 carbon atoms (C10), methyl trans-10-undecenoate ester, ethyl trans-10-undecenoate ester and the like each of which has 11 carbon atoms (C11), and dodecanoic acid and the like each of which has 12 carbon atoms (C12), or a salt or prodrug of the compound.
US20110129461 Mat II Beta Subunit RNAi and Therapeutic Methods Using Same The presently disclosed subject matter generally relates to methods and compositions for modulating MAT II activity. More particularly, the presently disclosed subject matter relates to methods and compositions for inhibiting the expression of MAT II β subunit in a subject via RNAi by administering siRNA or shRNA molecules directed to MAT II β subunit. In some embodiments, the methods and compositions of the presently disclosed subject matter generally relates to the treatment of cancer. More particularly, the methods and compositions of the presently disclosed subject matter relates to the inhibition of MAT II β subunit for the treatment of leukemia.
CN101768126B Novel triazole antifungal compound and salt thereof The invention relates to technical field of medicine, in particular to novel azole antifungal compound and salt thereof and the application, wherein, X presents hydroxyl or straight-chain ester group or branch-chain ester group with 1-6 carbon atoms and the ester group with easily-leaving group; Y presents substituent group on aromatic ring; M presents propargyl group or cyanomethyl; P presents various substituent groups on benzene ring, the substituent positions can be different positions on aromatic ring, mono substitution, or polysubstitution combined by the substituent groups; Z presents C or N atom; if Z presents Z atom, the position can be different positions on ring, and can be mono substitution, or polysubstitution; n is equal to 0-5; the salt comprises hydrochloride, nitrate, hydrobromide or methane sulfonate. The advantages of the invention are as follows: the compound provided by the invention has strong antifungal activity, low toxicity, and wide antifungal spectrum, and can be used for preparing novel antifungal drugs.
WO2009152189A1 Low dose topiramate/phentermine compostion and methods of use thereof A method for effecting weight loss by administering a combination of topiramate and phentermine is provided. The phentermine is generally administered in immediate release form, in a daily dose in the range of 2 mg to 8 mg, in combination with a daily dose of topiramate selected to prevent the loss of effectiveness of phentermine alone. Methods for treating obesity, conditions associated with obesity, and other indications are also provided, as are compositions and dosage forms containing low doses of phentermine and topiramate, e.g., 3.75 mg phentermine and 23 mg topiramate.
CN101157717B Preparation method of Ardisia mamillata B and uses thereof The invention pertains to the pharmaceutical technical field, which relates to a preparation method and the usage of ardisia mamillata B, the invention takes the whole trees or branches and leaves or roots and rhizomes of the ardisia mamillata as the medicines, the water, methanol water solution with an arbitrary proportion, ethanol water solution or organic solvent are used for extraction, the extract liquid is filtered and concentrated; the concentrate is prepared by recrystallization and refining after the independent or combined separation by macroporous resin, column chromatography(alumina or silica gel). The invention has the advantages that: the invention provides the preparation method of ardisia mamillata B which can be used for anti-tumor, anti-inflammation, analgesia, anti-virus (such as, influenza viruses, herpes viruses, hepatitis viruses, anti-retroviral viruses including HIV and so on), the cost is low, the process is stable, the yield is more than 1 percent of the dry herbs, the invention can obtain the ardisia mamillata B with high purity which has been removed a large amount of impurities, and the pharmacological activity is significant.
US8163754 Purine derivatives for use as adenosine A-2A receptor agonists Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
EP1280779B1 New polycyclic indanylimidazoles with alpha2 adrenergic activity The invention provides a compound of formula (I), wherein R1 to R3, -A-, m and t are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as alpha2 adrenergic agent.
CN101164621B Super-paramagnetic composite particle drug-loaded body and preparation method thereof The present invention relates to a superparamagnetic composite microparticle medicine-carrying body which can be mainly used for making magnetic target therapy and its preparation method. The inventedmagnetic composite microparticle medicine-carrying body is composed of magnetic composite microparticle and medicine-carrying layer which can be used for covering exterior of said magnetic compositemicroparticle. Said invention is characterized by that it utilizes the property of high surface activity of gold shell layer or colloidal gold of superparamagnetic composite microparticle to directlycover medicine or firstly utilizes the property of high surface activity of the gold shell layer or colloidal gold of superparamagnetic composite microparticle to make its surface be covered with high-molecular material, then utilizes the affinity adsorption or covalent linkage of high-molecular material to medicine to cover the medicine, also can make the surface of superparamagnetic composite microparticle be covered with the high-molecular material and medicine cross-linked or target preparation and medicine cross-linked or high-molecular material, target preparation and medicine cross-linked composite body layer.
US20090239841 Diaryl Ureas as CB1 Antagonists Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
CN103301432A Drug for treating lamb crazy The invention belongs to the field of medicines, and particularly relates to a medicine for treating lamb crazy. The medicine is prepared from ruddle, cassia twig, dalbergia wood, uncaria, rhizoma zingiberis, rheum officinale, honey-fried licorice root, grass yam, born keel, raw oyster shell, amethyst, donkey-hide gelatin, tortoise plastron glue, deer-horn glue, gypsum rubrum, red halloysite, plaster stone and talcum powder as materials. The materials are cleaned and put in a ventilated sunny place to air or dry in the sun, and grinded into 120 meshes of fine powder. The drug has the advantages of being good in treatment effect, short in treatment course, free of toxic and side effect, low in treatment cost, and the like.
CN101073562A Instant taurine eyes gel The invention is concerned with the method of preparation for the 1000ml. instant taurine ophthalmic gelatin. It contents: taurine 5-50g, antiseptic 0.05-1g, osmoregulation 1.0-7.5g, gel substrate 30-150g, and the certain amount of acid-base buffer and injection usage water to fulfill the requested weight of the medicine. The invention enriches the pharmaceutical dosage form of the taurine that prolongs the residence time of the medicine at the eye areas, and improves the curative effect with no negative stimulation.
WO2007002973A3 Use of stilbene derivatives for the production of medicaments for the treatment of solid tumours The invention relates to the use of stilbene derivatives of general formula (I), for the production of medicaments for the treatment of solid tumours, such as melanomas, or stomach cancers. In addition to the anti-tumour activity of the single substance, furthermore, acceptable results can be achieved by means of the combination dosing of a DNA-intercalating substance such as dacarbazine with stilbene derivatives of formula (I).
EP1534260A2 Perfluorinated fatty acids for the treatment of obesity, diabetes, hyperlipidaemia, cancer and inflammation A perfluoroctanoic acid or a salt or an ester thereof, perfluorosuberic acid, perfluoroheptanoic acid, perfluorohexanoic acid, perfluoropentanoic acid, perfluorobutanoic acid or perfluoropropionic acid or a salt or an ester any thereof, or perfluoroctane are useful in treating diabetes, obesity, hypercholesterolaemia, hyperlipidaemia, cancer, inflammation or other conditions in which modulation of lipid or eicosanoid status or function may be desirable.
WO2011091461A1 Compounds for use in the treatment of diseases The present invention relates to a compound of general formula (III) for use in the treatment and/or prevention of diseases, in particular inflammatory diseases, which are related to eosinophile peroxidase, wherein R1 is CH2, NH, O, S or a single bond, R2, R3, R4, R5 and R6 independently of one another are H, OH, F, Cl, Br, I or a C1 to C5 alkyl group, and R7 is H, OH, NH2, NH-NH2 or CH3.
CN103446120A Application of Fluevirosines A in preparation of anti-platelet aggregation drug The invention relates to application of Fluevirosines A in preparation of an anti-platelet aggregation drug. The application of the Fluevirosines A in the preparation of the anti-platelet aggregation drug is disclosed for the first time. Due to the fact that the skeleton type is a novel skeleton type, the Fluevirosines A has outstanding substantive characteristics and meanwhile has a remarkable improvement in platelet aggregation inhibition obviously.
DE102004032823A1 New D-xylopyranosyl-substituted phenyl compounds are sodium-dependent glucose cotransporter inhibitors useful to prevent or treat e.g. diabetes mellitus, complications of diabetes, metabolic acidosis or ketosis D-Xylopyranosyl-substituted phenyl compounds (I) and tautomers and/or stereoisomers and salts are new. D-Xylopyranosyl-substituted phenyl compound of formula (I) and tautomers and/or stereoisomers and salts are new. either R1 : H, F, Cl, Br, 1-6C alkyl, 2-6C alkynyl, 2-6C alkenyl, 3-7C cycloalkyl, 3-7C cycloalkyl-1-3C-alkyl, 5-7C cycloalkenyl, 5-7C cycloalkenyl-1-3C alkyl, 1-4C alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, aminocarbonyl, 1-4C alkylaminocarbonyl, di-(1-3C alkyl)aminocarbonyl, pyrrolidin-1-ylcarbonyl, piperidin-1-ylcarbonyl, morpholin-4-ylcarbonyl, piperazin-1-ylcarbonyl, 4-(1-4C- alkyl)piperazin-1-ylcarbonyl, 1-4C alkoxycarbonyl, amino, 1-4C alkylamino, di-(1-3C alkyl)amino, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl, piperazin-1-yl, 4-(1-4C alkyl)piperazin-1-yl, 1-4C alkylcarbonylamino, 1-6C alkyloxy, 3-7C cycloalkyloxy, 5-7C cycloalkenyloxy, aryloxy, 1-4C alkylsulfanyl, 1-4C alkylsulfinyl, 1-4C alkylsulfonyl, 3-7C cycloalkylsulfanyl, 3-7C cycloalkylsulfinyl, 3-7C cycloalkylsulfonyl, 5-7C cycloalkenylsulfanyl, 5-7C cycloalkenylsulfinyl, 5-7C cycloalkenylsulfonyl, arylsulfanyl, arylsulfinyl, arylsulfonyl, OH, CN or NO2 (where the alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl partly or completely fluorinated or mono- or disubstituted by identical or different substituents of Cl, OH, 1-3C alkoxy or 1-3C alkyl; in cycloalkyl and cycloalkenyl, 1-2 methylene is replaced by O, S, CO, SO or SO2 and in N-heterocycloalkyl, a methylene is replaced by CO or SO2); R2 : H, F, Cl, Br, OH, 1-4C alkyl (mono- or polysubstituted by F), 1-4C-alkoxy, CN or NO2; R3 : R1, (hetero)aryl or heteroaryloxy; and R4, R5 : H, F, Cl, Br, I, CN, NO2, 1-3C alkyl or 1-3C alkoxy (methyl or methoxy substituted by 1-3F); or CR1R2, CR3R4 : phenyl ring; or R1R2, R3R4 : 3-5C alkylene or 3-5C alkenylene bridge, which may be partly or totally fluorinated or mono- or disubstituted by Cl, OH, 1-3C alkoxy or 1-3C alkyl and where 1-2 methylene groups are replaced by O, S, CO, SO, SO2 or N-Rb; Rb : H or 1-4C alkyl; L : F, Cl, Br, I, 1-3C alkyl, CF2, CF3, 1-3C alkoxy, OCF2, OCF3 or CN; R7a, R7b, R7c : H, (1-8C alkyl)carbonyl, (1-18C alkyl)oxycarbonyl, arylcarbonyl or aryl-(1-3C alkyl)-carbonyl; X : H, 1-6C alkyl, 2-6C alkynyl, 2-6C alkenyl, 3-7C cycloalkyl, 3-7C cycloalkyl-1-3C alkyl, 5-7C cycloalkenyl (1-3C alkyl), aryl(1-3C alkyl), heteroaryl(1-3C alkyl), 1-4C alkylcarbonyl, arylcarbonyl, aminocarbonyl, 1-4C alkylaminocarbonyl, di-(1-3C-alkyl)aminocarbonyl, (aryl-1-3C-alkyl) aminocarbonyl, pyrrolidin-1-ylcarbonyl, piperidin-1-ylcarbonyl, morpholin-4-ylcarbonyl, hydroxycarbonyl, 1-4C alkoxycarbonyl, 1-4C alkylcarbonylamino-1-3C alkyl, N-(1-4C alkylcarbonyl)-N-(1-3C-alkyl)-amino-1-3C-alkyl, arylcarbonylamino-1-3C alkyl, 1-4C alkylsulfonylamino-1-3C alkyl, arylsulfonylamino-1-3C alkyl, 1-6C alkoxy-1-3C alkyl, 3-7C cycloalkyloxy-1-3C alkyl, 5-7C-cycloalkenyloxy-1-3C alkyl, aryloxy-1-3C-alkyl, heteroaryloxy-1-3C-alkyl, 1-4C alkylsulfanyl-1-3C-alkyl, 1-4C alkylsulfinyl-1-3C alkyl, 1-4C alkylsulfinyl, 1-4C alkylsulfonyl, 1-4C alkylsulfonyl-1-3C alkyl, 1-4C arylsulfanyl-1-3C alkyl, arylsulfonyl-1-3C alkyl, aryl-1-3C alkyl-sulfonyl-1-3C alkyl, 1-4C alkylsulfonyloxy- 1-3C alkyl, arylsulfonyloxy-1-3C alkyl, aryl-1-3C-alkyl-sulfonyloxy-1-3C alkyl, 3-7C-cycloalkylsulfanyl-1-3C alkyl, 3-7C-cycloalkylsulfinyl, 3-7C-cycloalkylsulfonyl, 5-7C-cycloalkenylsulfanyl-1-3C alkyl, 5-7C-cycloalkenylsulfinyl, 5-7C-cycloalkenylsulfonyl, 1-4C alkylcarbonylsulfanyl-1-3C alkyl or CN (where the alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl partly or totally fluorinated or mono- or disubstituted by Cl, CN, OH, mercapto, 1-3C alkoxy or 1-3C alkyl; and in cycloalkyl or cycloalkenyl, 1-2 methylene groups are replaced by O, S, CO, SO or SO2; and in N-heterocycloalkyl, methylene is replaced by CO or SO2); and Z : O, methylene, dimethylmethylene, difluoromethylene or carbonyl. Provided that X representing hydroxymethyl group is excluded and where the aryl represents phenyl or naphthyl optionally mono- or disubstituted by L; the heteroaryl (opti
US20110098302 Cyclic diaryl ether compounds as antagonists of prostaglandin d2 receptors Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
US7759070 Conserved inner core lipopolysaccharide epitopes as multi-species vaccine candidates A conserved inner-core oligosaccharide epitope expressed on the lipopolysaccharide (LPS) of a range of disease causing pathogenic bacterial isolates, including Actinobacillus pleuropneumoniae (Ap), Mannheimia haemolytica (Mh) and Pasteurella multocida (Pm), is disclosed. Construction of a mutant bacterial strain exclusively expressing the conserved inner core OS epitope as a terminally exposed structure has allowed the identification, production and isolation of an inner core LPS which is common to all three organisms. Further provided are associated vaccines, antibodies raised against the conserved LPS inner core and glycoconjugates comprising the LPS inner core linked to an immunogenic carrier.
US20080317875 Inhibitor of PI3 kinase-dependent inflammatory cytokine synthesis and method for inhibiting the same The present invention provides a novel inhibitor for inhibiting synthesis of a PI3 kinase-dependent inflammatory cytokine in vivo in a vertebrate and a method for inhibiting the same. More particularly, the present invention provides a suppressor for suppressing a cell-mediated immune response and a method for suppressing the same, as well as an activator for activating a humoral immune response and a method for activating the same. In the present invention, by administering Li ion to a living body to inhibit synthesis of an inflammatory cytokine, a cell-mediated immune responses can be suppressed, and immune-mediated inflammatory disorders (IMIDs) can be treated.
CA2165297C Myeloid cell leukemia associated gene mcl-1 A gene, mcl-1, of the bcl-2 family is disclosed along with its nucleotide and amino acid sequence. Also disclosed are diagnostic and therapeutic methods of utilizing the mcl-1 nucleotide and polypeptide sequences.
CN101091715A Composition of medication for treating cardiovascular diseases and cerebrovascular diseases The present invention relates to a medicine composition for curing angiocardiopathy and cerebrovascular disease. Said medicine composition contains ginsenoside and breviscapine.
US7625904 Methods for the treatment of sleep disorders The invention relates to methods for the treatment of a sleep disorder in a mammal comprising administering to said mammal an effective amount of a compound of formula (I): wherein all variables are as defined herein.
CN1823809A Preservative less water soluble vitamin preparation for injection and its formulating method A vitamin preparation soluble in the water for injection and without antiseptic is proportionally prepared from VB1, VB2, VB12, VB6, VC, folic acid, nicotinamide, glycine, sodium pantothenate, NaCaEDTA, etc through proportional mixing, filtering for removing bacteria, pouring in containers, freeze drying, plugging, and covering.
WO2006081794A1 Dietary food The invention relates to dietary food, especially in the form of dietary drinks, deserts, bars, soups, sauces, and pastries, the fatty acids contained in said food being essentially natural fatty acids with a chain length of up to C 18, essentially in the form of free fatty acids or the salts thereof and bonded as monoglycerides, and the free fatty acids bonded as monogylcerides are at least partially saturated and/or monoethenoid fatty acids. The invention also relates to a fatty acid mixture, especially for producing dietary food, the fatty acids contained therein being essentially natural fatty acids with a chain length of up to C 18, essentially in the form of free fatty acids or the salts thereof and bonded as monoglycerides, and the free fatty acids bonded as monogylcerides are at least partially saturated and/or monoethenoid fatty acids. The invention further relates to the use of an inventive fatty acid mixture, to food to which an inventive fatty acid mixture is added, and to the use of the inventive food for feeding patients with food-related illnesses and illnesses caused by disturbance of the absorption, the decomposition or the elimination of certain dietary components or the secondary products thereof.
WO2011027805A1 Therapeutic agent for mood disorders Disclosed is a therapeutic and/or prophylactic agent for mood disorders, which contains a thiazole derivative represented by general formula (I) (wherein R1 represents an aryl group or the like, and R2 represents a pyridyl group or the like) or a pharmaceutically acceptable salt thereof as an active ingredient.
US20050234015 Low molecular weight heparin salt with triethanolamine useful as therapeutic-antitrombotic agent of local delivery, procedures for preparing them, process for elimination of hygroscopicity of heparin salt, pharmaceutical compositions for local use in antithrombotic therapy and uses therein Low molecular weight heparin salt with triethanolamine useful as a therapeutic-antithrombotic agent for local delivery, having at least 60% of its total mass a molecular weight of less than 8000 Da and an average molecular weight from 4000 to 6000 Da, said salt also having a content of organic sulfur from 6.1 to 7.5 weight % (theoretical 6.8%) and a triethanolamine content from 42.6 to 52.1 weight % (theoretical 47.4 weight %). The processes for preparing the heparin salt, eliminating hygroscopicity of said salt, and pharmaceutical compositions for use in local antithrombotic therapy and its uses are also disclosed.
CN101336993A External tincture for treating wind-dampness arthralgia and urgent sprain and preparation method thereof The invention relates to a tincture medicament for external administration, which cures rheumatic arthralgia and acute sprain and contusion symptoms. Every 1000 ml of the tincture medicament for external administration is mainly prepared from the following raw materials by the weight ratio: 18 to 28 g of coral ardisia root, 18 to 28 g of Photinia serrulata, 18 to 28 g of cortex periplocae, 18 to 28 g of zanthoxylum nitidum DC, 18 to 28 g of glabrous sarcandra herb, 0.5 to 0.8 g of camphor, 12 to 19 g of giant knotweed rhizome, 6 to 10 g of securdaca inappendiculata hassk and 0.5 to 0.8 g of borneol. Compared with the 'bonesetting liquid', the tincture medicament has almost the same curative effects of eliminating wind, expelling pathogentic cold from channel, promoting blood circulation, eliminating stasis, detumescence and alleviating pain, furthermore, the raw materials thereof are widely and easily available, and the main active components of each medicinal material in the formula can be effectively extracted and preserved; the tincture medicament product has no obvious toxic or side effect, and the administration is safe and convenient, thereby enriching the medicament variety for curing rheumatic arthralgia and acute sprain and contusion symptoms.
US20060074125 Novel dithiolopyrrolones with therapeutic activity The present invention provides novel dithiolopyrrolone compounds and their salts, which are useful as treatments for cancer and other proliferative diseases. The present invention also provides therapeutic compositions comprising particularly useful types of dithiolopyrrolones, the salts thereof, and methods of using the compounds within such types, particularly in treating proliferative diseases such as cancer.
CN1935124A Tetramethylpyrazine phosphate slow-release micro-pill and its preparing method The present invention relates to the field of medicine preparation, in the concrete, it relates to a ligustrazine phosphate slow-released micropill and its preparation method. Said preparation is formed from two kind of slow-released micropills with different medicine-releasing actions, so that the medicine can be quickly released so as to obtain a certain blood concentration.
WO2012146936A1 Pyrrolnitrin derivatives There is provided pyrrolnitrin derivatives of formula I for use in medicine, preferably for the treatment of cancer.
CN101637491B Health-care food having functions of assisting antidiabetics and assisting antiatheroscloresis, and preparation method thereof The invention discloses a health-care food having functions of assisting antidiabetics and assisting antiatheroscloresis, mainly made of propolis, balsam pear extract, ginkgo biloba leaf extract, chromium picolinate and olive oil according to a certain weight proportion. The health-care food can be prepared into as any one of the following forms for taking easily: hard capsule, tablet, oral liquid and particularly soft capsule. The health-care food can adjust internal secretion, promote the circulation of blood, reduce the viscosity of blood and has functions of assisting antidiabetics and assisting antiatheroscloresis.
WO2008144061A2 Novel combinations comprising a phosphodiesterase-5 inhibitor and their use The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiestersa-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.
US20060014754 Methods and compositions for treating diseases and conditions of the eye Methods for the prevention and treatment of diseases and conditions of the eye including, but are not limited to: central retinal artery occlusion; central retinal vein occlusion; optic neuropathy including, but not limited to, anterior ischemic optic neuropathy and glaucomatous optic neuropathy; and macular (dry) degeneration are disclosed. These methods comprise administering to a patient a prophylactically or therapeutically effective amount of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase type 5 inhibitor. Pharmaceutical compositions and dosage forms comprising cyclic guanosine 3′,5′-monophosphate phosphodiesterase type 5 inhibitors are also disclosed.
US20120115868 Novel triazole compounds ii The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A α5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
CN1748699A Albendazole new form for treating allergic rhinitis The present invention relates to the preparation process of nebula, aerosol, powder spraying agent and nose drop of albendazole and their application in treating allergic rhinitis.
CN102058564A Zaltoprofen slow-release/controlled-release preparation and preparation method thereof The invention relates to a novel preparation of non-steroid anti-inflammatory medicine zaltoprofen, namely a zaltoprofen slow-release/controlled-release preparation, and a preparation method thereof. The method comprises the steps of loading zaltoprofen in a blank pill core to obtain a zaltoprofen-loaded pill core with swift disintegration, namely a quick-release pellet, coating on the zaltoprofen-loaded pill core to obtain a zaltoprofen slow-release pellet, and loading the quick-release pellet and the slow-release pellet into a gastric soluble capsule. The zaltoprofen slow-release/controlled-release preparation provided by the invention has the advantages of mature preparation process, convenience in industrial production and stable quality, and can reduce adverse reactions of zaltoprofen, reduce medicine taking frequency and improve compliance of patients.
CN101254202A Gargle preparations containing diastatin nystatin The invention relates to a nysfungin mouthwash preparation for oral application and uses thereof. The nysfungin mouthwash preparation is prepared from nysfungin serving as an active ingredient and aromatic synergistic agents with synergetic effect can be added to the preparation. The mouthwash preparation is available in the form of mouthwash tablet, effervescent tablet, dispersible tablet, granule or buccal tablet. The inventive nysfungin mouthwash preparation can be used for preventing and treating oral fungal infections; and has the advantages of good therapeutic effect, low side effects, low irritation, and good medical prospect.
WO2007042912A2 Heterocyclic compounds as pstat3/il-6 inhibitors The present invention relates to novel heterocyclic compounds of the general formula (I), as IL-6 inhibitors, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and compositions, their metabolites and prodrugs thereof. The present invention more particularly provides novel heterocyclic compounds of the general formula (I). Also included is a method for treatment of cancer, cancer cachexia and inflammatory diseases including immunological diseases, particularly those mediated by cytokines such as IL-6, through pSTAT3 inhibition, in a mammal comprising administering an effective amount of a compound of formula (I) as described above.
WO2010040826A1 6-phenyl-pyrimidin-4-yl-(phenylamine or phenoxy) derivatives useful as modulators of nicotinic acetylcholine receptors This invention relates to novel 6-phenyl-pyhmidin-4-yl-(phenylannine or phenoxy) derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
US20080132476 Administering e.g. 17beta-Fluoro-9alpha-vinyl-estra-1,3,5(10)-triene-3,16alpha-diol to treat endometriosis, osteoporosis, or hormone replacement therapy in combination with other drugs This invention describes the new 9α-substituted estratrienes of general formula I in which R3, R7, R7′, R13, R16 as well as R17 and R17′ have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.
US20100137412 Lentivirus pseudotyped with influenza hemagglutinin and methods of use Highly effective pseudotyping of lentiviral vector with influenza HA, NA and M2 packaging gene constructs at the proper ratios. Lentivirus vector pseudotyped with influenza HA, especially pseudotyped with H5 and neuraminidase. Methods of inducing immune responses to influenza antigens or for transducing genes into cells to which influenza antigens bind using such lentivirus vectors. Methods for screening drugs which inhibit influenza infection using lentivirus pseudotyped with HA.
US7465741 selective serotonine (5-HT) reuptake inhibitor activity in combination with additional alpha 2-adrenocptor antagonist activity; To treat anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia without being sedative The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with at least one radical that is attached to the phenyl radical by a carbon-carbon bond as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherin all variables are defined in claim 1. (I) The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity in combination with additional α2-adrenocptor antagonist activity and show a strong antidepressant and/or anxiolytic activity and/or antipsychotic and/or a body weight control activity without being sedative. Also, in view of their selective serotonine (5-HT) reuptake inhibitor as well as α2-adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.
US20110319471 Lna antagonists targeting the androgen receptor The invention relates to oligonucleotide compounds (oligomers), which target androgen receptor mRNA in a cell, leading to reduced expression of the androgen receptor. Reduction of the androgen receptor expression is beneficial for the treatment of certain disorders, such as a hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of androgen receptor using said oligomers, including methods of treatment.
CN1579390A Extenal preparation of phentolamine mesylate The invention relates to a new preparation method for methane sulfonate phentolamine. The preparation includes 10mg-2g per tablet of methane fulfonate phentolamine, the preparation can be effervesce tablet, suppository, jelly, atomization agent, or external preparation using curry as base material. The preparation applies to treatment of male erection function trouble and female sexless state.
WO2009079405A3 Assessing treatment compliance This document provides methods and materials related to determining whether or not a mammal is receiving a steroid treatment. For example, methods and materials involved in assessing a biological sample (e.g., a urine sample) from a mammal for the presence or absence of a steroid or a steroid metabolite to determine whether or not the mammal is complying with a steroid treatment (e.g., a corticosteroid treatment for an allergic disease or asthma) are provided.
WO2010151160A1 O-substituted 3-n-heteroaryl-1,3,4-oxadiazolones for medical use The present invention relates to compound of formula (I), wherein A represents a 5- or 6-membered heteroaromatic ring system containing up to 4 heteroatoms selected from O, S and N, which is optionally substituted, and to a stereoisomer, pharmaceutically acceptable salt or ester, or prodrug thereof.
US7915246 Milnacipran; sub-class of dual serotonin norepinephrine reuptake inhibitors characterized by a non-tricyclic structure and inhibit the reuptake of norepinephrine to an equal or greater extent than they inhibit the reuptake of serotonin; with gabapentin, pregabalin; no phenylalanine, tyrosine, tryptophan The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.
US20080268012 Extracted demineralized bone matrix having osteoinductive activity Demineralized bone matric (DBM) and native bone morphogenetic protein (nBMP) are complex mixtures of non-collagenous bone proteins. These mixtures contain many of the BMPs that are available as recombinant molecules. Information regarding the presence in these materials of molecules that may affect the availability and activity of the BMPs is very limited. A chemical extraction of DBM, such as using alkali-urea produces a water soluble extractate which inhibits the osteogenic activity of DBM. Noggin, an extracellular BMP ligand antagonist is found in the water soluble extractate from DBM. Differential chemical extraction is a useful means of removing non-osteogenic, or osteogenic inhibitory molecules from DBM and nBMP.
CA2535614C Quinazoline analogs as receptor tyrosine kinase inhibitors This invention provides quinazoline analogs of Formula (I): where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 groups. The invention also includes methods of using compounds of Formula (I) as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
US20100310609 Compositions and methods for treatment of neurodegenerative diseases Provided are electrokinetically-altered fluids (gas-enriched electrokinetic fluids) comprising an ionic aqueous solution of charge-stabilized oxygen-containing nanostructures in an amount sufficient for treating an inflammatory neurodegenerative condition or disease (e.g., multiple sclerosis (MS), Parkinson's disease (PD), Alzheimer's disease (AD)) or at least one symptom thereof. The electrokinetically-altered fluids or therapeutic compositions and methods include electrokinetically-altered ionic aqueous fluids optionally in combination with other therapeutic agents. Particular aspects provide for regulating or modulating intracellular signal transduction associated with said inflammatory responses by modulation of at least one of cellular membranes, membrane potential and/or conductance, membrane proteins such as membrane receptors, including but not limited to G-Protein Coupled Receptors (GPCR), and intercellular junctions (e.g., tight junctions, gap junctions, zona adherins and desmasomes). Other embodiments include particular routes of administration or formulations for the electrokinetically-altered fluids (e.g., electrokinetically-altered gas-enriched fluids and solutions) and therapeutic compositions.
CN102574824A Desferrithiocin polyether analogues and uses thereof Desferrithiocin analogues represented by the structural formulae described here, such as formula (I), are useful in treating conditions such as metal overload (e.g., iron overload from transfusion therapy), oxidative stress, and neoplastic and preneoplastic conditions.
CN102266324B New application of kappa-opioid receptor agonist The invention discloses an application of kappa-opioid receptor agonists U50 and 488H in preparation of drugs for treating diabetes. In the invention, the good blood sugar reducing effect of kappa-opioid receptor agonists U50 and 488H is creatively discovered, and the research shows that the blood sugar reducing mechanisms of kappa-opioid receptor agonist U50 and 488H are as follows: (1) increasing the level of skeletal muscle adiponectin receptor 1 (AdipoR1) and enhancing the sensitivity of adiponectin and insulin; (2) promoting the membrane translocation of glucose transporter (GLUT4) in skeletal muscle cell and increasing the glucose transport capability of the skeletal muscle cell; and (3) promoting the activation of AMPK (adenosine-monophosphate-activated protein kinase) in the skeletal muscle cell and enhancing insulin sensitivity. In the invention, a new option is provided for the preparation of the drugs for treating diabetes.
WO2012031993A1 Novel n-hydroxy-benzamides for the treatment of cancer The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.
US20090291986 Composition and method of treating facial skin defect This invention relates to a subcutaneous deliverable composition containing an agonist of the peroxisome proliferator-activated receptor-gamma, and a method for treating facial skin defects in a mammalian subject using the subcutaneous deliverable composition.
US7326710 Aralkyl formyl-alkyl piperazine derivatives and their uses as a cerebral nerve protective agent Aralkyl formyl alkyl piperazine derivatives Pharmaceutical compositions comprising the same, and methods of using them as a neuroprotective agent. Pharmaceutical results indicate that these compounds have excellent neuroprotective activities and fewer side effects.
US20090280088 Method of controlling hair shape The present invention provides a method for determining or modulating hair morphology and properties of natural wavy and frizzy hair and a method for evaluating or selecting a hair morphology modulator. The present invention provides a method for modulating hair morphology, including controlling an expression of IGFBP-5 gene or IGFBP-5 protein in a human hair follicle.
US20080014175 Methods and Compositions for Viral Enhancement of Cell Killing The present invention is directed to novel methods of enhancing the effectiveness of DNA damaging agents by exposing cells to viruses prior to or during exposure to the damaging agent. In certain embodiments of the invention, the DNA damaging agent is ionizing radiation, the virus is an adenovirus, and the increase in cell killing is synergistic when compared to radiation alone.
WO2012165398A1 Cycloalkyloxybiaryl compound The present invention relates to a compound having an excellent DGAT inhibitory activity and an anti-feeding activity or a pharmacologically acceptable salt thereof. A compound represented by general formula (I) [wherein R represents a phenyl group which may be substituted by 1-5 groups independently selected from substituent group (A), or the like; Q represents a nitrogen atom, or a group represented by the formula -CH=; U represents a nitrogen atom, or a group represented by the formula -CH=; V represents a nitrogen atom, or a group represented by the formula -CH=; m represents 0 or 1; and n represents 0 or 1; wherein the substituent group (A) consists of a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C1-C6 alkoxy group and so on], or a pharmacologically acceptable salt thereof.
EP0988108B1 superporous hydrogel composites having fast swelling, high mechanical strenght, and superabsorbent properties A superporous hydrogel composite is formed by polymerizing one or more ethylenically-unsaturated monomers, and a multiolefinic cross-linking agent, in the presence of particles of a disintegrant and a blowing agent. The disintegrant, which rapidly absorbs water, serves to greatly increase the mechanical strength of the superporous hydrogel and significantly shortens the time required to absorb water and swell. Superporous hydrogel composites prepared by this method have an average pore size in the range of 10 mu m to 3,000 mu m. Preferred particles of disintegrant include natural and synthetic charged polymers, such as cross-linked sodium carboxymethylcellulose, cross-linked sodium starch glycolate, and cross-linked polyvinylpyrrolidone. The blowing agent is preferably a compound that releases gas bubbles upon acidification, such as NaHCO3. Improved hydrogel composites formed without a blowing agent are also provided.
US20080221185 Psychoses, dementia or attention deficit disorder; 2-[3-(4-chlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl]-N-[2-(methyloxy)phenyl]acetamide The invention provides a compound of formula (I) or a solvate thereof: wherein R1, R2, R3, R4, R5, R6, and n are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
WO2011125836A1 Therapeutic agent or prophylactic agent for fibromyalgia Disclosed is a therapeutic agent or prophylactic agent that has analgesic effects on both nociceptive pain and neuropathic pain and is effective in the treatment of fibromyalgia. Specifically disclosed is a therapeutic agent or prophylactic agent for fibromyalgia that includes, as an active component, a cyclohexane derivative represented by the formula, or a pharmaceutically acceptable salt or prodrug thereof.
CN103230452A Trauma paste and preparation method of trauma paste The invention discloses a trauma paste and a preparation method of the trauma paste. The trauma paste comprises the following raw materials in parts by weight: 90-110 parts of garden burnet, 90-110 parts of raw rhubarb, 90-110 parts of raw rhizoma atractylodis, 90-110 parts of calamine, 45-55 parts of beewax, 990-1100 parts of sesame oil and 4-6 parts of borneol. The trauma paste disclosed by the invention has the functions of relieving pains and eliminating swelling, removing rots and generating tissues, clearing heat and removing toxicity, astringing and resisting bacteria and is good in treatment effects on burns, empyrosis, various traumatic skin infections or deep skin tissue ulcers which are not cured for a long time.
US7902253 Isoflavone derivatives of tectorigenin, the preparation thereof and the antiviral medicine containing the same as an effective constituent An isoflavone derivative of tectorigenin compound as shown in formula (II), its preparation method and the antiviral medicine containing it as an effective constituent. The compound structure is shown as follows: Where:: R1 is H, NH2 or SO3M; R2 is OR′; R3 is H or —CH2NR″; where R′ is H, —CH2COONa or —CH2CH2NMe2; NR″ is or —NMe2; M is H, Na, K or N+H (CH2CH2OH)3.
CN102603712A S-type and R-type tetrahydro-naphthalene amides antitumor compound and pharmaceutically acceptable salt or pro-drug thereof, preparation method and application The invention relates to a novel compound R1 represented by general formula I. The compound R1 is an S-type or R-type tetrahydro-naphthalene amides compound, or a pharmaceutically acceptable salt or pro-drug of the compound, and is used as an antitumor drug. The invention also provides a preparation method of the compound, and a pharmaceutical composition containing the compound, and an antitumor research in vitro. The antitumor drug R1 obtained by the invention is the S-type or R-type tetrahydronaphthalene amides compound, is better in antitumor activity and safety and can be applied to treating tumors such as leukemia, lung cancer, liver cancer, colon cancer and ovarian cancer, so that the therapeutic window is wide, and the compound as an antitumor agent in the medicine field is very valuable.
EP1084125B1 Condensed thienopyrimidines with phosphodiesterase-v inhibiting action The invention relates to thienopyrimidines of the formula (I) and their physiologically compatible salts, where R1, R2 and X have the meanings given in claim 1. These thienopyrimidines have a phosphodiesterase-V inhibiting action and can be used for the treatment of cardiovascular diseases and for the preventive and/or curative treatment of impotence.
WO2012055880A1 Method of treatment based on atad2 inhibitors A method of treating autoimmune and inflammatory diseases or conditions in a mammal, such as a human, which comprises the administration of an inhibitor of the bromodomain-containing protein: ATAD2.
CN101461787B Preparation method of hydroxycamptothecin nano crystal lyophilized powder for injection preparation The invention discloses a method for preparing a nanometer hydroxycamptothecin crystal freeze-dried powder preparation. Main raw materials of the nanometer hydroxycamptothecin crystal freeze-dried powder preparation consist of an active raw material, namely hydroxycamptothecin, phospholipids, a surfactant, namely poloxamer 188 or polyethylene glycol stearate-15, and a freeze-dried auxiliary material excipient. The method for preparing the nanometer hydroxycamptothecin crystal freeze-dried powder preparation comprises the following steps: after the hydroxycamptothecin is added into an alkalinesolution to be dissolved, the phospholipids are added in an ultrasonic water bath, and the poloxamer 188 or the polyethylene glycol stearate-15 is added into the mixture under magnetic stirring to bedissolved; the pH value of glacial acetic acid is adjusted to be between 4.0 and 6.0, and hydroxycamptothecin crystals are precipitated; and then the high-pressure homogenization is performed to obtain a nanometer hydroxycamptothecin crystal suspension, and then the freeze-dried auxiliary material excipient is added to be freezely dried to obtain the nanometer hydroxycamptothecin crystal freeze-dried powder preparation. The method is simple and easy to operate. Nanometer crystal freeze-dried powder has the advantages of high dispersity, good stability and so on. The average size of the crystals is 355.6nm, the average content of the hydroxycamptothecin in a sample is 98.5 percent of labeled amount, and the effect of inhibiting and killing liver cancer and gastric cancer cells of the preparation is remarkably stronger than that of a hydroxycamptothecin injection.
CN103566346A Drug for treating elderly abdominal distension and preparation method thereof The invention discloses a drug for treating elderly abdominal distension. The drug comprises 6-14 parts of ginseng, 10-20 parts of bighead atractylodes rhizome (fried), 5-15 parts of licorice (processed with honey), 10-20 parts of rhizoma cyperi (processed with vinegar), 12-18 parts of citron, 6-14 parts of amomum fruit, 13-17 parts of elecampane, 10-20 parts of fructus aurantii (stir-baked with bran), 14-22 parts of pericarpium citri reticulatae, 25-35 parts of semen raphani (fried), 8-16 parts of medicated leaven (fried), 10-20 parts of malt (fried), 14-22 parts of hawthorn (fried), 8-16 parts of gizzard pepsin (fried), 9-15 parts of inula flower, 26-34 parts of ruddle, 5-15 parts of ginger processed pinellia, 9-21 parts of pawpaw, 9-21 parts of dendrobe, 14-26 parts of yam, 10 parts of ginger and 15 parts of jujube. The preparation method of the drug comprises the following steps: firstly, decocting ruddle in a boiler to boil, wrapping the inula flower in cloth, mixing the components, adding 3 times of water to soak the components for 30 minutes, and then, putting the components in the boiler, boiling the components through strong fire, and continuing to decoct the components for 30 minutes through slow fire, removing residues, extracting juice, continuously decocting the components for twice, mixing the decoction obtained in twice to obtain the drug. The components mutually act, thereby both curing the stomach and protecting the stomach, treating both manifestation and root cause of disease, facilitating to create gastrointestinal digestion and promoting reinforcement of gastrointestinal motility.
US20080064647 A polyvalent multimeric complex formed from a plurality of circularly permuted chimeric pRNA molecules, each carrying a stabilized biologically active moiety; degradation resistant stabilized ribozyme is correctly folded such that it remains intracellularly active A polyvalent multimeric complex formed from a plurality of circularly permuted chimeric pRNA molecules, each carrying a stabilized biologically active moiety.
US20100279978 Methods of reducing the severity of mucositis The invention provides methods of reducing the severity of mucositis, involving administration of a toll-like receptor 4 antagonist.
US20090143474 Reduced dose intravenous acetaminophen Described herein are compositions and methods for intravenous administration of acetaminophen at a single dose level of less than about 1000 mg for the treatment or prevention of pain (e.g., postoperative pain) and/or fever.
CN103417513A Compound containing Lafutidine and preparation containing Lafutidine The invention relates to a compound containing Lafutidine and a preparation containing Lafutidine. The compound comprises Lafutidine, lactose, tween-80, hydroxypropyl cellulose and talcum powder. Compared with the prior art, the compound is evidently faster in capsule dissolution rate and low in impurity content. In addition, the results of various detection of the compound meet the specification.
CN101297841B Compound Tripterygium wilfordii multi-glycosides formulation for curing rheumatic disease and preparation method thereof The invention relates to a compound tripterygium glycoside preparation for treatment for rheumatic diseases and a preparation method thereof. The invention takes tripterygium glycoside and artemether as main drugs and is in combination with pharmaceutical excipients, microcrystalline cellulose, lactose, low-substituted hydroxyproxyl cellulose, tiny powder silica gel and magnesium stearate for preparing tablets. The weight ratio is that: 5g of tripterygium glycoside and 5 to 30g of artemether. The invention proposes to allow the tripterygium glycoside and the artemether to be compatible to realize the synergy of the efficacies, and the compatibility of the tripterygium glycoside and the artemether has higher treatment effects on rheumatic diseases than that of the tripterygium glycoside.
CN1939539A Local prescription for wart, nail-disease treatment and nail care An anhydrous medicine for treating wart and nail disease by local application and nursing nail contains one or more active components, the carrier chosen from lactic acid, malic acid, tartaric acid, citric acid and C14 alkyl hendecanate (or undecenate), and the physiologically chosen auxiliary. Its preparing process is also disclosed.
US20120021071 Use of a synergistic combination of hypothiocyanite and/or hypohalite ions and lactoferrin for preparing a treatment for cystic fibrosis The invention relates to the use of a synergistic combination of at least one ion selected from the group including hypothiocyanites and/or hypohalites and of lactoferrin for preparing a pharmaceutical composition for treating cystic fibrosis. In one embodiment, the lactoferrin is one having a purity higher than 95% and substantially free of lipopolysaccharides, endotoxins, and angiogenins, and having an iron saturation level higher than 15%.
CN101245002B Process for producing steady iodination vegetable oil, iodination vegetable oil fatty acid ethyl ester The invention relates to a method for preparing stable iodized vegetable oil and iodized vegetable oil fatty acid ethyl ester, which includes the following steps: first, vegetable oil and iodized hydrogen gas are caused to take addition reaction so as to generate iodized vegetable oil; then, the unstably combined iodine in iodized vegetable oil is removed by heating and ventilating air method, and the removed free iodine is eliminated by using lopsidedness sulfite solution liquid sealing, thus getting the iodized vegetable oil with good stability; the stable iodized vegetable oil and ethanol are caused to take transesterification reaction under the effect of salt catalyst so as to generate the stable iodized vegetable oil fatty acid ethyl ester. The product prepared by the method for preparing stable iodized vegetable oil and iodized vegetable oil fatty acid ethyl ester has the advantages of low viscosity, good stability and low cost.
CN103664880A Novel anticoagulation medicine and preparation method and application thereof The invention provides a novel anticoagulation medicine and hydrate and/or solvate thereof, wherein n is 1, 2, or 3. The invention further provides a preparation method of hydrate and/or solvate of the novel anticoagulation medicine, and an application of the novel anticoagulation medicine in preparing a medicine for treating and preventing thrombus.
US20130023575 Compositions and methods for the treatment of ocular surface allergies The disclosure provides ophthalmic compositions, systems and methods for the treatment of ocular surface allergies. More particularly the present invention relates to compositions of bromfenac for the treatment of the signs and symptoms of ocular surface allergies due to seasonal allergies.
WO2013119917A1 Materials and methods for treating diarrhea The present invention provides therapeutic compositions and methods for treating gastrointestinal diseases and conditions such as diarrhea, for providing rehydration, for correcting electrolyte and fluid imbalances, and/or for improving small intestine function. In one embodiment, the present invention provides a composition formulated for enteral administration, wherein the composition does not contain glucose. In a preferred embodiment, the composition is formulated for administration as an oral rehydration drink.
CN102558130A 2-(4-fluorine phenyl)-3-nitryl-8-ethyoxyl-2H-benzopyran chiral compound and preparation method and application thereof The invention relates to a 2-(4-fluorine phenyl)-3-nitryl-8-ethyoxyl-2H-benzopyran chiral compound and a preparation method and the application thereof and specifically discloses a ((R)-XM002S (formula I)) and an (S)-XM002S (formula II) of the chiral compound and the preparation method of the chiral compound. The application of the chiral compound in preparation of anti-tumor medicine is further disclosed.
CN101579459A Medicine for treating hyperosteogeny and diskal hernia and preparation method The invention relates to a medicine for treating the hyperosteogeny and the diskal hernia and a preparation method thereof. Bindwood, hemlock parsley, angelica, radix linderae, radix angelicae pubescentis and asarum, which are respectively of 20 to 40 grams, eucommia bark and achyranthes, which are respectively of 25 to 35 grams, safflower, coralbean bark, teasel root, lycopodium calvatum, lopseed, notoginseng, mastiche, myrrh and dragon's blood, which are respectively of 10 to 20 grams, 5 to 8 pieces of woodlouse, 2 to 5 pieces of chilopod and 2 to 4 grams of borneol are respectively dried, pulverized and uniformly mixed, and then are proportioned into paste by 45 percent of ethanol to be sealed and stored for standby use. When needs to be used, the medicine is pasted on an afflicted part. The medicine has the advantages of simplicity, high effectiveness and thorough treatment.
EP2123266A1 Cancer therapeutic agent and anti-carcinogenic agent Provided is a carcinogenesis suppressing agent, cancer therapeutic agent, or agent for mitigating adverse reactions of anticancer agents, which is ingestible on a daily basis and with low prevalence of adverse reactions, comprising a reduced coenzyme Q as an active ingredient. The agents are useful as pharmaceuticals, cosmeceutical, cosmetics, foods such as functional foods (supplements, health aid foods, nutritional supplementary foods, nutrient-fortified foods, nutrient-adjusted foods, health beverages, foods for specified health uses, foods with nutrient function claims), animal drugs, animal feeds, or animal foods.
CN103656291A Medicine for treating pharyngitis and preparation method thereof The invention discloses a medicine for treating pharyngitis and a preparation method thereof. The medicine is mainly prepared from the following medicines by weight: coptis chinensis, rhizoma phragmitis, poria cocos, honeysuckle, moutan barks, common hogfennel roots, blackberry lily and the like. The medicine disclosed by the invention has the functions of clearing away heat and toxic materials, decreasing internal heat and dissolving phlegm and moistening lung and dissolving phlegm, and is quick in effect, good in curative effect and free from replase for treating pharyngitis.
CN101897880A Liquor for detoxifying and maintaining kidney The invention discloses a manufacturing method of liquor for detoxifying and maintaining kidney. The manufacturing method is characterized by comprising the following steps of: cutting a pig kidney with a knife, cutting the pig kidney into crisscrosses, putting into a hot pottery pot and boiling for 10 minutes with liquor, then adding chest polygonum posumbu, gypsum, ginseng, Fushen, anemarrhena, scutellaria, the root of kudzu vine, liquorice, Mongolian snakegourd root and block soybean, boiling for 20 minutes by adding 1: 0.25 river water, then adding magnetite, crystal sugar, white and yellow wines respectively with a half pot, sealing the pot for 15 days, taking out and removing residues to obtain the finished liquor. The liquor prepared by adopting the method can achieve a certain effect while a patient takes within seven days.
WO2014108168A1 Piperidinylcarbazole as antimalarial The present invention provides compounds of Formula (I) for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases. Formula (I) wherein R3, R4, X and Y have the meaning given in claim 1.
CN102166219A Nasal administration preparation and application thereof The invention provides a nasal administration preparation which takes an antisense oligonucleotide medicament flutide (of which the sequence is 5'-CCTTGTTTCTACT-3') as a main component and is used for preventing and treating H1N1, H3N2 and H5N1 influenza virus infection, belonging to the field of chemical pharmacy. The nasal administration preparation takes the flutide as an effective component and also contains a proper amount of preservatives, buffer solution and medicinal auxiliary materials, and the pH value of the preparation is 7-8. The preservatives are reagents which can not influencethe physicochemical properties of medicaments and have no harm to human bodies, no irritation and no special odor under the inhibitory concentration. Common preservatives comprise methyl paraben, ethyl paraben, propyl paraben, butyl paraben, ethyl hydroxy benzoate, potassium sorbate, benzoic acid, benzalkonium bromide, chlorhexidine acetate, o-phenyl phenol, eucalyptus oil, cassia oil, peppermintoil and the like. The flutide nasal administration preparation has no irritation and very low toxicity, and is a medicament which has a high action speed and a lung targeting function when used for treating influenza.
US20100125100 GOLD NANOROD-siRNA COMPLEXES AND METHODS OF USING SAME Provided are methods and compositions for inhibiting expression of one or more target genes. The compositions contain RNA polynucleotides that can inhibit expression of a target gene via RNA interference (RNAi) electrostatically complexed with surface functionalized gold nanorods (GNRs). The RNA polynucleotides are not covalently bound to the surface functionalized GNRs. The method involves inhibiting expression of a target gene in an individual. The method is performed by administering to the individual an effective amount of a composition containing surface functionalized GNRs electrostatically complexed with RNA polynucleotides, such as siRNA, that can inhibit expression of the target gene via RNAi. The siRNA is not covalently bound to the surface functionalized GNRs.
EP2203453A1 Pyrazolo[5, 1-c] [1,2,4]triazines, methods for preparation and use thereof A pyrazolo[5,1-c][1,2,4]triazine compound of Formula (A): and pharmaceutically acceptable sats thereof. The multiply-substituted pyrazolo[5,1-c][1,2,4]triazine compounds of the invention selectively inhibit B-Raf kinase activity and are useful for treating disorders mediated by B-Raf kinase.
CN101054393B Adefovir dipivoxil anhydrous crystal, preparation method and medicine composition thereof The present invention relates to adefovir dipivoxil anhydrous crystallisate, characterized in that: XRD: radiating with Cu-k alpha , x ray powder diffraction spectrum expressed in 2 theta having characteristic absorption peak at 3.2,6.5,8.6, 15.7,19.6,21.6, DSC: DSC converting due to absorbing heat at 80 degree; infrared absorption spectrum : KBr pellet , characteristic absorption peak being at 3287cm<-1>, 3175cm<-1>, 1753cm<-1>, 1254cm<-1>, 1147 cm<-1>, 1025cm<-1>, 970cm<-1>. The present invention also discloses adefovir dipivoxil anhydrous crystallisate preparation method and its pharmaceutical composition. The inventive adefovir dipivoxil anhydrous crystallisate dissolves quicker than 102 degree crystal form, is high in dissolution, and is stable relative to 94 degree crystal form and not easy to be hygroscopic.
US20080038331 Enantiomerically pure S-etifoxine, pharmaceutical compositions thereof and methods of their use Enantiomerically pure S-etifoxine and pharmaceutically acceptable salts, solvates, hydrates or prodrugs thereof are provided. Also provided are pharmaceutical compositions comprising the compounds and methods of treating disorders associated with central nervous system using the compounds and pharmaceutical compositions.
CN102600132A Oral preparation containing amisulpride The invention relates to an oral preparation containing amisulpride. The amisulpride which is active medicine is prepared into cyclodextrin inclusion compound, is sieved, is uniformly mixed with pharmaceutically acceptable auxiliary materials, and is granulated by a wet method or a dry method, obtained granules are squashed to form tablets, filled into capsules to form a capsule preparation or is directly separately packaged to obtain a granule preparation. The water solubility and the stability of the oral preparation containing the amisulpride can be strengthened, bitter taste of the amisulpride is covered, medication compliances of patients are improved, and bioavailability of the oral preparation is improved to a great extent.
US20110009480 Biologically active taxane analogs and methods of treatment The present application relates to new taxane analogs, pharmaceutical compositions comprising such analogs and methods of treating cancer comprising such compositions. The compounds according to the present application have the general formula: wherein R1 and R2 are each selected from H, alkyl, alkenyl or aryl; R3 is hydroxyl or OP1; R4 is OH or R7COO; R7 is alkyl, alkenyl or aryl, R8 and R9 are each independently selected from H, alkyl or alkenyl. The compounds of the present application may particularly be 9,10-α,α-OH taxane analogs that are formed by a process starting with a standard taxane as the starting compound.
CN1600297A Loratadine paster of penetrating skin A transdermal disk of loratadine for treating allergic disease is prepared from loratadine, adhesive aggregate, cross-linking agent, plasticizer, solvent and smosis promoter through proportionally mixing.
US20090306040 Mono and Combination Therapy of M1/M4 Agonist (Sabcomeline) for Treatment of Negative Symptoms of Schizophrenia The invention relates to the use of a functional muscarinic M1/M4 receptor agonist or a pharmaceutically acceptable salt thereof for the treatment of negative symptoms of schizophrenia. It also relates to adjunctive and simultaneous combination therapies for the treatment of negative symptoms of schizophrenia in which the functional muscarinic M1/M4 receptor agonist or a pharmaceutically acceptable salt thereof, in particular sabcomeline or a pharmaceutically acceptable salt thereof and at least one neuroprotective agent, neuroleptic and/or atypical antipsychotic agent are administered adjunctively or simultaneously. The invention also provides methods of treatment of the negative symptoms of schizophrenia utilising such therapies and such adjunctive or simultaneous therapeutic combination therapies, therapeutic combinations for use therein and pharmaceutical compositions comprising them.
CN101574344A Niacin and statin medicinal composition and preparation method thereof The invention provides a niacin and statin medicinal composition and a preparation method thereof. The composition comprises a niacin sustained-release tablet core, a statins coating layer and a protective layer, and is characterized in that: the statins coating layer comprises statins, polyvinyl alcohol-polyethylene glycol grafted copolymer or butyl hydroxy anisol. The preparation method comprises the following steps: firstly preparing a niacin sustained-release tablet; taking the tablet as a tablet core, attaching a coating layer containing the statins on the tablet core, and coating one or more layers of gastric-soluble film coatings on the coating layer containing the statins; and preparing the niacin and statin medicinal composition by taking the statins of coating fluid containing the statins as main medicaments, the polyvinyl alcohol-polyethylene glycol grafted copolymer as a main coating material, the butyl hydroxy anisol as an antioxidant, and ethanol solution containing water as solvent.
CN102488654A Drug for curing periodontitis The invention relates to a drug for curing periodontitis, which is used for solving the problems of being incapable of permeating in a deep part of a periodontal pocket, poor in curative effect and inconvenient for drug delivery in the traditional drug for curing periodontitis. The drug for curing periodontitis comprises the following components in parts by weight: 5-250 parts of doxycycline, 25-1000 parts of metronidazole, and 10000 parts of glycerol. According to the invention, two kinds of antibiotics which are broad-spectra antibiotics are adopted; the two antibiotics are matched with each other so as to basically cover all bacteria in an oral cavity, so that the curative effect is definite; due to the good viscosity, the drug for curing periodontitis disclosed by the invention can stay in the periodontal pocket for a long time; due to the good flowability, the drug for curing periodontitis can be injected into the periodontal pocket by using a fine needle, so that patients cannot feel pain; the patients can apply the drug, so that the drug of the patients can be delivered everyday can be ensured; and the drug concentration in the periodontal pocket can be effectively kept, thus, an obvious curative effect can be achieved.
US20120220556 Drospirenone for hormone replacement therapy A pharmaceutical composition comprising as a first active ingredient an estrogen, such as estradiol or estradiol valerate, in sufficient amounts to treat disorders and symptoms associated with deficient endogenous levels of estrogen in women, and as a second active ingredient 6β,7β;15β;16β-dimethylene-3-oxo-17α-preg-4-ene-21,17-carbolactone (drospirenone, DRSP) in sufficient amounts to protect the endometrium from the adverse effects of estrogen is useful for, amongst others, treating peri-menopausal, menopausal and post-menopausal women. This composition may be used for hormone replacement therapy and may be administered as a multi-phased pharmaceutical preparation. This combination therapy may comprise continuous, sequential or interrupted administration, or combinations thereof, of DRSP and estrogen, each optionally in micronized form.
WO2006035296A1 Process for the preparation of an orlistat derivative useful as reference standard in the determination of the purity of orlistat and process for the preparation of orlistat The invention relates to a leucine derivative, N-2[(S)-2-N-formylamino-4-methyl pentanoic acid (S)-1-[[3(S)-hydroxy-5-oxo-4-hexyl methyl]dodecyl ester] amino-4-methyl pentanoic acid (S)-1-[(2S, 3S)-3-hexyl-4-oxo-2-oxetanyl]methyl dodecyl ester of Formula (I), and process for isolating it. More particularly, it relates to the preparation of pure orlistat, which is (S)-2-Formylamino-4-methyl pentanoic acid (S)-1-[(2S, 3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester. The invention also relates to the use of the Compound of Formula (I) as reference standard or reference marker for checking the purity of orlistat.
US20120035253 Crystalline forms of genistein The disclosure relates to new crystalline forms of genistein. The disclosed crystalline forms include crystalline genistein sodium salt dihydrate; crystalline genistein potassium salt dihydrate; crystalline genistein calcium salt; crystalline genistein magnesium salt; crystalline genistein L-lysine salt; crystalline genistein N-methylglucamine salt; crystalline genistein N-ethylglucamine salt; crystalline genistein diethylamine salt; and crystalline genistein monohydrate. The disclosure also relates to the novel genistein salts represented by these crystalline forms. Therapeutic compositions containing at least one of these crystalline forms of genistein and/or a genistein salt and a pharmaceutically acceptable carrier are described. The disclosure also relates to methods of treating cancer comprising the step of administering to a patient in need thereof a therapeutically effective amount of a therapeutic composition containing the compounds of the disclosure, of a crystalline form of genistein, or of a genistein salt.
WO2005023782A1 Substituted fused pyrimidine-4(3h)-one compound A compound represented by the general formula (I): (I) [wherein A is phenyl, etc.; R1 is R1a (R1a is substituted alkyl, etc.), -Z1b-R1b (R1b is substituted alkyl, etc. and Z1b is -NH-, etc.), -Z1c-R1c (R1c has the same meaning as R1b or is alkyl and Z1c is -C≡C-, etc.), -N(R1b)(R1c), etc.; R2 and R3 each is hydrogen, optionally substituted alkyl, OH, etc.; R4 and R5 each is hydrogen, optionally substituted alkyl, OH, etc.; X is OH or alkoxy; and Y is optionally substituted alkyl, etc., provided that when Y is a specific group and A is phenyl, then R4 and R5 each is hydrogen and -C(CF3)2(X) is -C(CF3)2(OH) bonded to the phenyl group in the 3- or 4-position thereof] or a pharmacologically acceptable salt or ester of the compound. They are highly active in bonding to LXR and are useful as a medicine for warm-blooded animals (especially for the human), preferably as a medicine for treatments for and/or prevention of arteriosclerosis, hyperlipemia, inflammatory diseases, diabetes, etc.
US7485623 administering 4-hydroxy tamoxifen percutaneously to a patient having dense breast tissue; 4-hydroxy tamoxifen may be formulated in a hydroalcoholic gel or an alcoholic solution A method of treatment comprises administering 4-hydroxy tamoxifen percutaneously to a patient having dense breast tissue. The 4-hydroxy tamoxifen may be formulated in a hydroalcoholic gel or an alcoholic solution.
US7670606 Method for administering a vaginal care composition A vaginal care composition is introduced directly into the vagina in the form of an ovule, a cream or an ointment or with a tampon or which is brought into a position outside the vagina on a panty liner. The composition comprises viable Lactobacillus or Bifidobacterium microorganisms, non-viable Saccharomyces cultures, saccharide(s), vitamin A, and zinc.
US20120190732 Multifunctional Aptamer-Nucleic Acid Nanostructures for Tumor-Targeted Killing The present invention provides compositions comprising a ligand-nucleic acid nanostructure that promote tumor cell-specific killing and methods of using the compositions. Specially, the invention provides aptamer-nucleic acid nanostructures for treating tumors in a mammal. The methods of making the compositions are also provided.
EP1910313A1 6-thioamide substituted benzimidazoles The invention relates to (6)-thioamide-substituted benzimidazoles of formula (1), in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.
CN103479896A Medicament for treating cerebral thrombosis and preparation method of medicament The invention discloses a medicament for treating cerebral thrombosis and a preparation method of the medicament. The medicament is prepared mainly from astragalus, angelica sinensis, ligusticum wallichii, prepared rehmannia root, rhizoma atractylodis, wolfiporia extensa, ginseng, rhizoma arisaematis, uncaria tomentosa and scorpion according to a certain weight proportion. The medicament disclosed by the invention has effects of promoting the circulation of qi, relieving stagnation, dispelling the wind, removing spasm, dredging collaterals and relieving collaterals blood, is used for treating cerebral thrombosis, has a short treatment course and a high response speed, has no relapse phenomenon after a patient is healed, and has no toxic or side effects.
US20090136489 Methods for the treatment, diagnosis, and prognosis of cancer We have discovered that antizyme inhibitor (AZI) is expressed at increased levels in highly proliferating cells. We have also discovered that inhibiting antizyme inhibitor, including inhibiting its expression, reduces the growth of cancer cells. The present invention is directed to the use of inhibitors of antizyme inhibitor for the treatment of cancer, the use of antizyme inhibitor for the diagnosis and prognosis of cancer, and methods for identifying novel cancer treatments.
US7029692 content of monoterpene ketone in the nicotine-containing layer is 0.1 to 5.0%-wt of the weight; masks the unpleasant smell of nicotine A transdermal therapeutic system having a backing layer, at least one nicotine-containing layer ore zone, which may have pressure-sensitive properties, as well as a removable protective layer is characterized by a content of at least one essential oil extracted from a mint species, or at least one monoterpene ketone contained in these essential oils.
US20080280903 antiapoptosis agents such as 1-[2-Methoxyimino-2-(4-pyrrolidin-1-yl-phenyl)-ethyl]-quinolinium bromide, used for cytoprotection or for side effect reduction of anticarcinogenic agents The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.
US20080107603 Administering L-ergothioneine; Alzheimer's disease, multiple sclerosis, stroke, traumatic brain injury, spinal cord injuries The present invention relates in general to methods of protecting a mammalian central nervous system cell from damage, and to methods of treating or ameliorating neurodegenerative diseases. The invention further relates to screening for neuro-protective agents that may alone, or in combination with other neuroprotective agents, aid in protecting cells of the central nervous system from damage attributed to neurotoxic compounds, free radicals, or neurodegenerative diseases. The invention further relates to pharmaceutical compositions comprising L-ergothioneine or other newly identified compounds and pharmaceutically acceptable carriers for administration to a mammal in need of neuroprotection.
CN102813649A Application of anisodine hydrobromide in preparing medicines for treating depression The invention discloses application of anisodine hydrobromide in preparing medicines for preventing or treating depression, in order to develop a medicine for effectively preventing or treating depression. Anisodine has the chemical formula of C17H21NO5 and a relative molecular weight of 319.35, is a pyrethroid type alkaloid, is present in belladonna plants and is a choline receptor blocking agent isolated firstly in China. The hydrobromide of the anisodine is mainly used clinically, and can be used for treating vascular headache, retinal vasospasm, central retinopathy, ischemic optic neuropathy, acute paralysis, paralysis agitans, bronchial asthma, kinesia, organic phosphorus pesticide poisoning and the like. However, literatures reporting treatment of depression are not available. In the invention, experiments show that anisodine hydrobromide plays a role in treating depression, and has a very good therapeutic effect in depression symptoms of interest blank, pleasant sensation disappearance, reduced exiting degree, reduced increment of body weight and the like.
US20080287532 Oxacyclopentene-2 derivatives The present invention relates to oxacyclopentene-2 derivatives as compounds possessing antiinflammatory, neuroprotective, immunomodulatory and cardiovascular activities in mammals.
US20080300262 Combination Therapy for Relief of Pain The present invention relates to analgesic compositions comprising a non-peptidyl N-type calcium channel blocker, and at least one other analgesic compound, and to methods of using N-type calcium channel blockers in combination with at least one other pain-relieving compound that alleviates pain through a mechanism other than N-type calcium channel blockage, or with a non-pharmacological therapeutic protocol.
WO2013116065A1 Novel morpholinyl derivatives useful as mogat-2 inhibitors The present invention provides compounds of Formula I or a pharmaceutical salt thereof, methods of treating hypertriglyceridemia using the compounds; and a process for preparing the compounds.
CN103393632A Cabazitaxel drug composition and preparation method thereof The invention provides a drug composition of cabazitaxel and a pharmaceutically acceptable biological carrier and a preparation method thereof. The cabazitaxel drug composition is actually a nanoparticle colloid dispersing system containing cabazitaxel. Cabazitaxel is encapsulated in a polymer shell made of proteins or is associated with the proteins by way of association to form nanoparticles, wherein the mass ratio of the cabazitaxel to the proteins is 1:(8-15); the pH value ranges from 5.0 to 7.0; the average diameter of the particles is not more than 200nm; the Zeta potential ranges from minus 10mv to minus 30mv; and the particles can be subjected to sterile filtration. The composition can be prepared by a high-pressure homogenating method or a protein denaturation and renaturation method. The composition prepared by the invention can be transformed to re-dispersable cakes or powder, can maintain stability for at least 48 hours at 37 DEG C after being re-dispersed in an aqueous medium, and can meet the requirements of intravenous drip therapy.
US20100130480 Benzoquinoline inhibitors of vesicular monoamine transporter 2 The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof.
CN103356602A Application of Chukrasone B in medicines for resisting osteoporosis caused by estrogen deficiency The invention discloses new application of Chukrasone B in preventing and treating osteoporosis. Osteoporosis is one of important diseases jeopardizing human health; and as the aging of population, osteoporotic patients increase progressively and bring about huge social, medical and economic burdens. Although related specialists and scholars at home and abroad attach great importance to osteoporosis, no effective therapeutic medicine can treat the disease. The in-vivo test detects that the Chukrasone B has obvious effect on resisting osteoporosis. The experimental result indicates that the Chukrasone B can inhibit the bone conversion rate enhancement caused by ovariectomy and cause less destruction of bones, and can also enhance the blood calcium concentration, thereby being beneficial to bone deposition. The Chukrasone B has therapeutic action on osteoporosis caused by estrogen deficiency, and does not have estrogen-like side effect.
CN103446054A Liposome combination drugs, industrial production process of liposome combination drug through molecular dispersion method, and quality control According to the invention, a liposome combination drug injection and an oral liposome combination drug preparation can be produced in a large industrialization manner through a molecular dispersion method with a unified formula, a unified process and unified equipment. The invention provides a formula of raw components for preparing liposome combination drugs in a molar ratio, provides freeze-drying injection and oral preparation processes for the prepared liposome combination drugs, and also provides twenty embodiments for preparing the liposome combination drugs, such as an anti-gastric-ulcer liposome combination drug, antibacterial and antifungal liposome combination drugs, an anti-tumor liposome combination drug, an anti-virus liposome combination drug, an anti-emetic liposome combination drug, a nutritional supplement liposome combination drug and hypoglycemic agent and cardiovascular medicine liposome combination drugs.
US7605155 Enzyme inhibitors from pyrazolo[1,5a]pyrimidine as enzyme inhibitors; cyclin dependent kinases (CDKs) inhibitors; cancer, inflammation and arthritis; neurodegenerative diseases such Alzheimer's; cardiovascular, viral and fungal diseases In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. All illustrative compound is shown below:
WO2010107115A1 Glycine transporter inhibitor Provided is a novel compound or a pharmaceutically acceptable salt thereof, which is useful for preventing or treating diseases attributed to glycine uptake inhibitory activity such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (such as generalized anxiety disorders, panic disorders, obsessive-compulsive disorders, social anxiety disorders, post-traumatic stress disorders, specific phobia, and acute stress disorders), depression, drug dependence, convulsion, tremor, and sleep disorders. The compound is represented by formula [I].
CN102038923A Medicament for treating dandruff The invention discloses a medicament for treating dandruff, which contains the following components in part by weight: 3 to 5 parts of borax, 1 to 2 parts of salt, 3 to 5 parts of Chinese honeylocust fruit, 2 to 5 parts of edible white vinegar, 2 to 6 parts of Job's-tears kernel, 1 to 5 parts of mung bean, 2 to 3 parts of common cnidium fruit, 3 to 5 parts of clove, 2 to 5 parts of rhubarb, 4 to 5 parts of Szechuan lovage rhizome, 5 to 8 parts of dried orange peel, 2 to 5 parts of cowherb seed, 4 to 5 parts of dried ginger, 2 to 10 parts of ever spring, 5 to 8 parts of gentian root, 2 to 5 parts of black sesame, 5 to 7 parts of wild chrysanthemum, 3 to 5 parts of tribulus fruit, 2 to 5 parts of dense-fruit pittany root-bark, 2 to 5 parts of mugwort leaf, 3 to 5 parts of purslane herb and 3 to 8 parts of licorice root. The medicament combined by the components has the effects of clearing heat, tonifying qi and regulating endocrine dyscrasia, can radically treat the dandruff, and also has the effects of preventing alopecia, relieving itching and moistening scalp and fur.
WO2008140373A1 A liquid formulation for administering nicotine A pharmaceutical liquid formulation for delivering nicotine in any form to a subject by trans dermal uptake for treating tobacco dependence and similar conditions, said formulation being a medicated body lotion, medicated body balm or medicated body gel. Also contemplated is a method for delivery of nicotine, a method for the reduction of the urge to smoke or use tobacco as well as methods for manufacturing said liquid formulation, the use of said liquid formulation for obtaining trans dermal uptake of nicotine through the skin of a subject, and use of nicotine for the production of a liquid formulation for the treatment of a disease selected from the group consisting of tobacco or nicotine dependence, Alzheimer's disease, Crohn's disease, Parkinson's disease, Tourette's syndrome and ulcerous colitis, and for post-smoking-cessation weight control.
WO2007068841A3 Use of a composition based on tretinoin, hydroquinone and fluocinolone acetonide, accompanied by a chemical peeling The invention concerns the use of a combination of hydroquinone, tretinoin, and fluocinolone acetonide for preparing a composition for preventing and/or reducing hyperpigmentary disorders associated with the application of a chemical skin peeling.
CN1565450A Naloxone Hydrochloride Injection and its preparation method The invention discloses a Naloxone hydrochloride injection and powder injection, and the process for preparation, wherein middle aperture fiber film hyperfiltration technology is employed to remove the impurities, thus diminishing the damage of main medicaments and improving the quality of products.
WO2008053517A1 Agent for promoting in vivo dha synthesis and seaweed oil It is intended to provide an agent for promoting in vivo DHA synthesis and a seaweed oil which enable the supplementation of DHA to a living body instead of taking oxidizable DHA as a fish oil. According to the agent for promoting in vivo DHA synthesis and the seaweed oil which contain fucoxanthin, even if oxidizable DHA is not taken as a fish oil, an activity of in vivo DHA synthesis can be increased by taking fucoxanthin or the seaweed oil containing fucoxanthin, whereby the supplementation of DHA to a living body can be substituted. Further, by adding this fucoxanthin or seaweed oil containing fucoxanthin to a food material, medicinal product or feed, the food material, medicinal product or feed which has a function to promote in vivo DHA synthesis can be provided.
CN1803133A Magnetic nanometer granule containing mitocin-C and its uses The invention provides magnetic nano particles containing mitomycin and its use, wherein the constituents comprise mitomycin C, polymeric compound and Fe3O4. The invention realizes the advantages of better dispersion in the system, small grain size and large specific surface area.
US7153526 Diagnosing bacteria infections; administering aqueou solution of silver colloids A method for combating bacterial infections affecting the gastrointestinal system of humans and animals is provided. The method is achieved by diagnosing a bacterial infection affecting the gastrointestinal system and periodically administering a dosage of concentrated aqueous pure ionic silver colloid to maintain a high level of pure ionic silver in the area to be treated over a period of time.
EP1394161B1 L-ascorbic acid-2-o-maleic acid-a-tocopherol diester 1-propanol adduct and process for producing the same L-Ascorbic acid-2-o-maleic acid-α-tocopherol diester 1-propanol adduct or its pharmacologically acceptable salt; cosmetic components, antioxidants, radical scavengers, antiinflammatory agents and elastase inhibitors containing the same as the active ingredient; and a process for producing the above-described adduct characterized by comprising extracting a solution containing L-ascorbic acid-2-o-maleic acid-α-tocopherol diester with a solvent, distilling off the solvent and adding to the residue 1-propanol optionally mixed with an organic solvent followed by crystallization.
US20110038930 Hot-melt extruded pharmaceutical dosage form The invention relates to a hot-melt extruded pharmaceutical dosage form with controlled release of a pharmacologically active ingredient (A) embedded in a matrix comprising a polymer (C), the dosage form exhibiting a breaking strength of at least 300 N and having an oblong shape comprising a longitudinal direction of extension, a transversal direction of extension orthogonal to the longitudinal direction of extension, a front side, an opposite back side and a circumferential rim between said front and back side; wherein the core of the pharmaceutical dosage form has a morphological orientation caused by hot-melt extrusion that is substantially orthogonal to the longitudinal direction of extension of the dosage form; and/or the release per area of the pharmacologically active ingredient (A) through the front side and the opposite back side is faster than the release through the circumferential rim.
WO2009080637A1 Compounds which potentiate the ampa receptor and uses thereof in medicine Compounds of formula (I) and salts thereof are provided: wherein n is 0, 1, 2 or 3; R1 is selected from phenyl and pyridyl, each of which is optionally substituted by one or two groups independently selected from C1-4alkyl and halogen; and R2 is selected from H and CH3 when n is 1 and R2 is H when n is 2 or 3. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
US20080132538 Pharmaceutical uses for fluoroalkoxybenzylamino derivatives of nitrogen containing heterocycles A method of treating overactive bladder disorders characterized by involuntary neurogenic detrusor contractions associated with the pathology of multiple sclerosis by administering fluoroalkoxybenzylamino derivatives of nitrogen containing heterocyclic compounds, and specifically, by administering compounds of the formula wherein Q, X1, X2 and X3 are as defined below, and their pharmaceutically acceptable salts.
CA2400377C Method for treating ocular pain The invention relates to the use of brimonidine for treating ocular pain.
WO2011069141A3 Interferon therapies in combination with blockade of stat3 activation Methods of modulating the INF-induced STAT3 activation in a patient in need- thereof are provided for the treatment of disease. The methods comprise the step of administrating to a patient the combination of a therapeutically effective amount of interferon including INF-α and/or INF-β in combination with a STAT3 inhibitor.
US20100260718 Irf-4 as a tumor suppressor and uses thereof The invention relates to methods for treating BCR/ABL mediated disorders. The methods of the invention also include monitoring progression of or sensitivity to treatment of BCR/ABL mediated disorders as well as identifying subjects for the treatment methods of the invention. Screening assays and related products and kits are also encompassed within the invention.
US20050260289 extracts from Lightyellow Sophora Root, Turmeric, Magnolia Bark, Moutan Bark extract, Isatis Leaf, Borneo Camphor Tree, Amur Cork Tree, Angelicae Dahuricae Root, Lemon, Smartweed extract, Licorice, Cnidii Rhizoma, Japanese Angelica Root extract, salicylic acid, resorcinol, alcohol, and water; eczema TECHNICAL FIELD: Lotion for therapy of dermatitis TECHNICAL PROBLEM: To provide a lotion for therapy effective against atopic dermatitis. MEANS FOR SOLVING: It has a composition: Lightyellow Sophora Root, 3%; Turmeric, 2%; Magnolia Bark, 2%; Moutan Bark, 2%; Isatis Leaf, 1%; Borneo Camphor Tree (Dryobalanops aromatica Gaertn.f.), 1%; Amur Cork Tree, 2%; Angelicae Dahuricae Root, 1%; Lemon, 3%; Smartweed, 2%; Licorice, 0.5%; Cnidii Rhizoma, 0.5%; Japanese Angelica Root, 0.5%; salicylic acid, 0.5%; resorcinol, 0.5%; alcohol, 30%; and water, 48.5%. A significant therapeutic effect against atopic dermatitis is obtained by a synergistic effect between antibacterial, antiviral, antiallergic, antiphlogistic, and blood-circulation accelerating actions as pharmacological effects of Lightyellow Sophora Root, Turmeric, Magnolia Bark, Moutan Bark, Isatis Leaf, Borneo Camphor Tree (Dryobalanops aromatica Gaertn.f.), Amur Cork Tree, Angelicae Dahurikae Root, Lemon, Smartweed, and Licorice, accelerating action for skin permeation and antifungal-sterilizing action of Cnidii Rhizoma and Japanese Angelicae Root, accelerating action for keratinization and antifungal-sterilizing action of salicylic acid and resorcinol, as described above. Principal Use: It is used for the therapy of dermatitis, particularly of atopic dermatitis.
CN102440994A Application of ganoderic acid G as immune synergist and super-antigen dependent therapeutic medicine in tumour treatments The invention relates to a novel purpose of ganoderic acid, in particular to application of the ganoderic acid G in various tumour treatments. The ganoderic acid G disclosed by the invention comprises various preparations including solid type preparations of troches, capsules and the like, ointment, pasting agents, injections and the like, which can be prepared by adopting a conventional method in a pharmaceutical field. The tumour treatment medicine provided by the invention, namely the ganoderic acid G, has the function of directly inhibiting tumour cell proliferation under small dose; at this time, the ganoderic acid G has low toxic effect on normal tissue cells; and the effect of further treating tumours is realized after adding super-antigen. The application of the ganoderic acid G as the immune synergist and the super-antigen dependent therapeutic medicine in the tumour treatments disclosed by the invention has the obvious advantages and the technical progresses that: when the ganoderic acid G is united with the super-antigen, the function of killing and wounding a wide variety of tumour cells in extracorporeal and esoteric experiments can be effectively played.
EP1763361A2 Steroid sparing agents and their use This invention relates generally to the use of a steroid sparing agent for the preparation of a medicament for the treatment of inflammatory bowel diseases (IBD), asthma, multiple sclerosis (MS), rheumatoid arthritis (RA), graft versus host disease (GVHD), host versus graft disease, and various spondyloarthropathies, comprising administering a steroid sparing immunoglobulin or small molecule composition to a patient in need thereof. The invention also relates generally to combination therapies for the treatment of these conditions.
US20120122810 Fused Pentacyclic Polyethers Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.
CN101972231A Dry suspension containing cefixime liposome and preparation method thereof The invention relates to cefixime liposome and preparation method therefore as well as dry suspension containing the cefixime liposome. The dry suspension is composed of the cefixime liposome and pharmaceutically acceptable carriers, wherein the cefixime liposome comprises the following components in parts by weight: 1 part of cefixime, 1.25-5 parts of hydrogenated soybean lecithin, 1.25-5 parts of hydrogenated yolk lecithin, 2.5-10 parts of cholesterol and 0.1-5 parts of polysorbate 80. The dry suspension not only accords with the requirements of Chinese pharmacopoeia, but also has the advantages of better storage stability in normal temperature, faster effect exertion and obviously improved bioavailability in comparison with the common cefixime medicaments.
CN101735215A Beta-carboline cyclosubstituted carbamide class raf kinase suppressor, preparation method and application thereof The invention relates to the field of pharmaceutical chemistry, in particular to a class of beta-carboline cyclosubstituted carbamide class compounds (I), a preparation method thereof, a medicinal composition containing these compounds and an application thereof in medical treatment, especially an application in the use of a raf kinase suppressor.
CN1727344A Derivant of cephalosporin of amidinothioacetamide, preparation method and application A C-3 chloroonium salt type cephalophytanic acid derivative or its pharmacologically acceptable salt is disclosed, which has high antibacterial activity to G+ bacterium and a certain antibacterial activity to enterococcus and G- bacterium. It is prepared by the reaction between 7-amino C-3 chloro 4-carboxyl cephalophytanic acid (7-ACCA) and bromoacetyl bromine or N,N bisubstituted thiourea.
CN101967153A Metabolite of 10-O-(dimethylamino ethyl) ginkgolides B and medicinal composition containing same The invention provides a compound, metabolite 10-O-(methylamino ethyl) ginkgolides B of 10-O-(dimethylamino ethyl) ginkgolides B and application of the metabolite 10-O-(methylamino ethyl) ginkgolides B in pharmacy. The structural formula of the metabolite 10-O-(methylamino ethyl) ginkgolides B is shown in the specification of the invention. Same as the raw material of the metabolite 10-O-(methylamino ethyl) ginkgolides B, the metabolite 10-O-(methylamino ethyl) ginkgolides B has the stronger function of resisting the collecting rate of platelet activating factor (PAF)-induced blood platelet and can be used for preventing and clinically treating ischemic stroke, inflammation, asthma and other diseases relevant to PAF factors.
CN103690483A Dl-praeruptorin A microemulsion and preparation method thereof The invention discloses a dl-praeruptorin A microemulsion and a preparation method thereof, and relates to dl-praeruptorin A microemulsions. The dl-praeruptorin A microemulsion comprises the following components by mass: 0.1%-0.8% of dl-praeruptorin A, 5%-10% of oil, 10%-16.67% of an emulsifier, 20%-33.33% of a co-emulsifier and the balance of water. The preparation method comprises the following steps: mixing the dl-praeruptorin A, the oil, the emulsifier and the co-emulsifier to obtain an oil phase, adding the water into the oil phase, uniformly mixing and emulsifying to obtain the dl-praeruptorin A microemulsion. The indissolvable drug-Pd-Ia (dl-praeruptorin A) is prepared into the O/W (oil/water) microemulsion by auxiliary materials with good biocompatibility, so that the solubility, the stability, the drug loading capacity and the transdermal absorption of the drug are improved. The prepared dl-praeruptorin A microemulsion is good in pereutaoeous permeation, low in skin irritation, simple in preparation process, low in cost and stable in quality, and has treatment and prevention effects on the cardiovascular disease, especially the coronary heart disease.
WO2011152755A1 Pharmaceutical composition for the treatment of disorders of the lower section of the urogenital system A pharmaceutical composition in the form of suppositories comprises a bioactive compound and a fatty base. The composition comprises, per suppository with a mass of 2.7 - 2.9 g: 0.050 - 0.500 g of glutamic acid, 0.025 - 0.250 g of lysine, 0.025 - 0.250 g of alanine, 0.025 - 0.250 g of arginine, 0.025 - 0.250 g of glycine, and 0.010 - 0.150 g (depending on the zinc content) of zinc in the form of zinc chloride. The composition can additionally contain 10 - 30 mkg of selenium in the form of anhydrous sodium selenite and 0.020 - 0.035 g of sodium fumarate.
CN103301473A Cis-platinum and gold nanoparticle hollow sphere shell carrier compound with light-operated releasing function and preparation method The invention relates to a cis-platinum and gold nanoparticle hollow sphere shell carrier compound with a light-operated releasing function based on a gold nanoparticle hollow sphere shell structure and a preparation method. The compound is in such a structure that a PEG link section is connected outside the gold nanoparticle hollow sphere shell and cis-platinum is connected through the PEG link section. Medicines are carried by means of the gold nanoparticle hollow sphere shell or a gold nanoparticle spherical structure with holes, and the surface of the gold nanoparticle sphere shell is modified by PEG with sulfydryl for connecting cis-platinum. Medicines carried by the gold nanoparticle sphere shell can be controlled to release through pulse laser.
WO2009016460A8 Pyrazole compounds and their use as raf inhibitors The present invention is directed to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.
WO2008104875A1 Oxazolidinones as cholesterol absorption inhibitors Novel oxazolidinones and pharmaceutical compositions are described, as are methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholeserolemia, and atherosclerosis.
CN102688319A Medicine composition granule for removing stasis The invention discloses a medicine composition granule for removing stasis, which is characterized by comprising the following raw materials of: rhubarb, angelica sinensis, akebia stem, fructus aurantii, cortex magnoliae officinalis, sappan wood, carthamus tinctorius L, dried orange peel, liquorice and mirabilite.
US20110129516 Ocular drug delivery devices A method of forming an ocular delivery device includes exposing a solid, shaped cellulose polymer to a solution including an active pharmaceutical ingredient (API) and a solvent capable of solubilizing the API, wherein the polymer absorbs at least a portion of the solution, including the API and solvent. The method may further include removing at least a portion of the absorbed solvent from the polymer by allowing the absorbed solvent to evaporate from the polymer or by drying the polymer. A variety of cellulose polymers may be used, including hydroxypropyl cellulose. A variety of APIs may be used, including Cyclosporine, Tobramycin and Vancomycin. Ocular delivery devices prepared by the methods may be used to treat a variety of eye disorders.
CN102247324A Flumazenil liposome injection The invention discloses a flumazenil liposome injection and a preparation method thereof. The liposome injection is prepared from flumazenil, cholesterol, phosphatidyl ethanolamine, soyasterol, tween 80, trehalose and polyvinylpyrrolidone in specific proportions by weight. The liposome injection disclosed by the invention has favorable preparation stability, the liposome can not be ruptured due to fusion, ice crystal and the like in the freezing process, and the liposome keeps the same favorable entrapment rate after long-term storage. The flumazenil liposome injection disclosed by the invention improves the solubility of flumazenil, improves the quality of the preparation product, reduces the toxic side effect, increases the retention time of the medicament in systemic circulation, improves the bioavailability of the medicament, obviously improves the curative effect, has a simple preparation method and is suitable for industrialized big production.
CN101002798A Sterilizing nebula for treating foot diseases, and its preparing method A medicine in the form of spray for preventing and treating beriberi and its complications is proportionally prepared from gamba, magnolol, menthol, borax, alcohol, urea and purified water through proportionally and respectively dissolving said raw materials in alcohol or purified water, mixing, stirring, solubilizing, filtering and loading in containers.
CN102861046A Application of Houttuynoid A in ovarian cancer treatment medicine The invention relates to application of Houttuynoid A in preparing an ovarian cancer treatment medicine, which belongs to the technical field of new application of the medicine. According to the assessment on the antineoplastic activity through in-vitro MTT method, Houttuynoid A has an obvious inhibiting effect on the growth of human ovarian cancer cell strains HO-8910, HOC1 and OVAC. Therefore, Houttuynoid A can be used for preparing the ovarian cancer treatment medicine, and has a favorable development and application prospect. The application of Houttuynoid A in preparing the ovarian cancer treatment medicine, which is provided by the invention, is disclosed for the first time, and because the skeleton type belongs to brand-new skeleton type, the inhibiting activity of Houttuynoid A to ovarian cancer cells is extremely strong.
WO2013175483A1 Process for preparing crystalline sorafenib tosylate The present invention provides an industrially suitable process for the preparation of substantially pure 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide or Sorafenib and its tosylate salt, with a suitable impurity profile and without requirement of any additional purification steps. The present invention also provides Sorafenib base (II) as stable crystalline Form-SSB. The present invention further relates to a process for the preparation of crystalline Sorafenib tosylate Form-I which is free from contamination of any other polymorphic form of Sorafenib tosylate, for e.g. Form II or Form III, and does not involve any seeding requirement for crystallization step.
CN101001862A Tricyclic compounds and their use as MGLUR1 antagonists In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's diseas.
WO2012070798A2 Topical antifungal composition comprising terbinafine or its salt The present invention provides a topical antifungal having excellent properties in skin penetration and retention in the skin. Specifically, the present invention provides a topical antifungal composition comprising terbinafine or its salt; a film-forming agent; a solvent; and one or more selected from the group consisting of urea, 1-dodecylurea, and 1,3-didodecylurea as an agent for increasing retention of terbinafine or its salt in an applied skin.
US20050208124 Drugs containing riboflavin-type compounds A medicament is provided containing as an active ingredient at least one of riboflavin, a riboflavin derivative or a pharmacologically acceptable salt thereof, which has the action of suppressing IL-1β, IL-6, IL-10, INF-γ, TNF-α, GM-CSF, IL-8, MCP-1 and other cytokines. Moreover, a preventative or therapeutic agent for inflammatory diseases accompanied by hypercytokinemia is provided which has excellent cytokine suppression effect.
CN102379888A Application of flavone glycoside compounds in preparing medicament for treating and preventing hepatitis The invention belongs to the field of pharmacy, and provides application of three flavone glycoside compounds luteolin-7-O-[alpha-L-rhamnose-(1->2)]-beta-D-glucoside (trivial name is lonicerin), apigenin-7-O-[alpha-L-rhamnose-(1->2)]-beta-D-glucoside (trivial name is rhoifolin) and luteolin-6-C-beta-D-glucose-8-C-beta-D-xyloside in preparing medicament or health-care food for preventing and treating hepatitis.
WO2005027883A1 Gsk-3 beta inhibitors in the treatment of bone-related diseases The present invention relates to methods for preventing and/or treating bone-related diseases in mammals, especially humans, using GSK-3ß inhibitors. The invention also concerns methods for selecting in vitro and/or in vivo compounds useful for preventing and/or treating bone-related diseases in mammals, including humans.
CN102580099A Composition for resisting ischemia reperfusion injury and preparation method and application thereof The invention relates to a medicinal composition for treating an ischemia reperfusion injury, particularly a hepatic ischemia reperfusion injury, and a preparation method and application thereof. The composition comprises an M-cholinergic receptor blocker and a cholinesterase inhibitor, has a simple and convenient preparation process, is safe to use, has an obvious curative effect, can be used for obviously improving the cell apoptosis caused by the ischemia reperfusion injury and overcomes the side effects caused by existing common medicaments. The invention expands novel medical application of an existing muscarinic receptor blocker and also provides a novel medicine intervention means for preventing and treating the ischemia reperfusion injury. The medicinal composition is suitable for large-scale production and commercial application in the industries of medicine, reagents and the like, has excellent application prospect and has obvious social benefits and economic benefits.
CN101721371A Cefetamet pivoxil hydrochloride submicron emulsion solid preparation and new application thereof The invention provides a cefetamet pivoxil hydrochloride submicron emulsion solid preparation, which comprises the following components in part by weight: 1 part of cefetamet pivoxil hydrochloride submicron emulsion grains, 0.4 to 3 parts of diluent, 0 to 0.5 part of disintegrating agent, 0 to 0.2 part of adhesive, 0 to 6 parts of flavoring agent, 0 to 0.4 part of aromatizer and 0 to 0.2 part of lubricant. The invention also discloses application of the preparation in preparation of a medicament for treating cholangitis, particularly acute pyogenic cholangitis.
EP2106793A1 Ready to use Oxaliplatin solutions Pharmaceutical composition comprises water, oxaliplatin and an acid, other than oxalic acid, whose anion does not impair the stability of the solution. An independent claim is also included for a pharmaceutical composition comprising water, oxaliplatin and more than 5 wt.% glucose. - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : None given.
EP1510518A2 Substituted 1,3,4-oxadiazoles and a method of reducing TNF-alpha levels Substituted 1,3,4-oxadiazole compounds reduce the levels of TNFα in a mammal. Typical embodiment are 2-[1-(3-cyclopentyloxy-4-methoxyphenyl)-2-(1,3,4-oxadiazol-2-yl)ethyl]-5-methylisoindoline-1,3-dione and 2-[1-(3-ethoxy-4-methoxyphenyl)-2-(1,3,4-oxadiazol-2-yl)ethyl]isoindoline-1,3-dione.
EP1270004B1 Use of gamma-tocotrienol as diuretic Diuretics, natriuretics, preventives/remedies for hypertension, preventives/remedies for ischemic heart diseases, preventives/remedies for congesitve heart failure or preventives/remedies for kidney diseases each containing η-tocotrienol.
CN102319210A Veterinary long-acting cefquinome sulfate injection and preparation method thereof The invention relates to the technical field of animal medicine, and particularly discloses veterinary long-acting cefquinome sulfate injection and a preparation method thereof. 100 mL of the injection comprises 2.5-7.5 g of cefquinome sulfate, 0.2-0.4 g of suspending agents, 0.4 g of bacteriostatic agents, 0.3 g of emulsion dispersants, and the balance of solvents. The preparation method comprises the following steps: firstly adding cefquinome sulfate into the solvent, stirring for well mixing; adding the suspending agent into the solvent with a temperature of 90-100 DEG C for dissolution; cooling the dissolved solution in the second step to room temperature, adding the suspension under stirring in the first step, uniformly stirring; adding the bacteriostatic agent and the emulsion dispersant in to the suspension in the third step, fully stirring; finally adding residual amount of the solvent, uniformly stirring, orderly adding the mixture into a high-speed shearing dispenser and a colloid mill, performing radiation sterilization to prepare the product. When the product is used in pigs by intramuscular injection, the elimination half life is long; the effective action time of themedicine in the body is prolonged; and the drug administration time is reduced.
US20100062059 S-Nitrosothiols Containing Composition for the Treatment of Fatty Liver Diseases, Obesity and Other Diseases Associated with the Metabolic Syndrome and the Use of Such Compositions The present invention refers to pharmaceutical compositions containing S-nitrosothiols as active principle. The referred compositions are intended for the treatment of the fatty liver disease and other diseases associated with the metabolic syndrome. The composition is administered either orally or rectally.
US7141583 Activity against both Gram-positive and Gram-negative pathogens are generally regarded as having a broad spectrum of activity Compounds of the formula (I), or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein HET is an N-linked 5-membered heteroaryl ring, optionally substituted on a C atom by an oxo or thioxo group; and/or by 1 or 2 (1–4C)alkyl groups; and/or on an available nitrogen atom by (1–4C)alkyl; or HET is an N-linked 6-membered heteroaryl ring containing up to three nitrogen heteroatoms in total, optionally substituted on a C atom as above; Q is selected from, for example, Q1 R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, of formula (TC5) wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
CN103142818A Multifunctional complex cleaning and treating prescription for women The invention discloses a multifunctional complex cleaning and treating prescription for women, and relates to the field of prevention and treatment of gynecological diseases. The multifunctional complex cleaning and treating prescription comprises the following six ingredients: topical antimycoin, topical antibacteriocin, a topical orifice antipyretic, a topical antihistamine, an acid-base equilibrium maintenance agent and a surface curing agent; the topical antimycoin includes menthol and multi-moldin; the topical antibacteriocin includes a garlic extract and neomycin; the topical orifice antipyretic includes eucalyptol, a cactus extract, sodium salicylate and sodium bicarbonate; the topical antihistamine includes menthol and phenergan; the acid-base equilibrium maintenance agent includes citric acid and sodium citrate; and the surface curing agent includes an aloe extract and a motherwort extract. By adopting the multifunctional complex cleaning and treating prescription for women, the normal power of hydrogen of the vaginal secretion can be maintained, and the pathogenic bacteria and the virus can be effectively prevented from growing.
EP1263413B1 Method of preparing solid dispersions The present invention is directed to improved methods for producing solid dispersions, especially pharmaceutical dispersions. These methods involve the dissolution of one or more insoluble or relatively insoluble substances, preferably pharmaceutically active substances, and/or one or more water-soluble substances, preferably carriers, in supercritical fluids and the subsequent removal of solvent by rapid expansion. These methods offer a number of advantages over traditional preparation methods and form formulations with highly desirable dissolution properties, especially for pharmaceuticals.
WO2007097961A1 Use of azurocidin inhibitors in prevention and treatment of ocular vascular leakage Provided are methods for alleviating a symptom of an eye condition by administering to a mammal an amount of azurocidin inhibitor effective to alleviate the symptom of the eye condition.
WO2013156329A1 Estrogenic components for use in the treatment of neurological disorders. The invention relates to the prophylactic and therapeutic applications of certain estrogenic components such as estetrol in neurological disorders such as neonatal hypoxic-ischemic encephalopathy (HIE).
WO2013139687A1 Method for administration of an anti tumor agent There is provided a new pharmaceutical product comprising Compound (A) characterized by a dosage regimen which maximizes anti-tumor activity while maintaining acceptable toxicity levels.
EP1562605A2 Compounds for modulation of cholesterol transport Methods for regulation of lipid and cholesterol uptake are described which are based on regulation of the expression or function of the SR-BI HDL receptor. The examples demonstrate that estrogen dramatically downregulates SR-BI under conditions of tremendous upregulation of the LDL-receptor. The examples also demonstrate the upregulation of SR-BI in rat adrenal membranes and other non-placental steroidogenic tissues from animals treated with estrogen, but not in other non-placental non-steroidogenic tissues, including lung, liver, and skin. Examples further demonstrate the uptake of fluorescently labeled HDL into the liver cells of animal, which does not occur when the animals are treated with estrogen. Examples also demonstrate the in vivo effects of SR-BI expression on HDL metabolism, in mice transiently overexpressing hepatic SR-BI following recombinant adenovirus infection. Overexpression of the SR-BI in the hepatic tissue caused a dramatic decrease in cholesterol blood levels. These results demonstrate that modulation of SR-BI levels, either directly or indirectly, can be used to modulate levels of cholesterol in the blood.
CN101397303A Sanggenole A compounds, preparation method and use thereof The invention discloses a new compound-mulberry-root hydroxybenzene A compound with the structure as shown in the formula (I). The invention further discloses a preparation method of the compound and the application of the compound in preparing medicines used for treating or preventing oral diseases, and preparing the oral caring products.
EP2323682A2 Compositions and methods for increasing serum antioxidant concentrations Compositions and methods are provided for increasing serum antioxidant levels, decreasing serum levels of oxidative chemical species, inhibiting insulin-receptor signaling activity, decreasing triglycerides levels, increasing serum ghrelin levels, and decreasing serum TNF-alpha levels. Compositions provided comprise a mixture of zinc- charged, fragmented proteins derived, for example, from serum or milk. Compositions are administered in a therapeutically effective amount to, for example, reduce oxidative stress levels in a mammalian subject.
US20120309787 Insulin-regulated aminopeptidase (irap) inhibitors and uses thereof The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.
EP1039804A4 Method for treating fibroproliferative disorders by inhibitors of protein hydroxylation The present invention relates to a method of treating conditions mediated by collagen formation together with cell proliferation by administering to a patient or living system an effective amount of a compound of Formulae (I) or (II) and derivatives thereof: R1, R2, R3 and R4 each individually represent a hydrogen, an alkyl, alkenyl, or alkoxy group containing 1 to about 8 carbon atoms, an aryl, aralkyl, or cycloalkyl group containing about 5 to 12 carbon atoms, or a carboalkoxy or carbamyl group containing up to 8 carbon atoms, or a peptide or peptidomimetic moiety containing 10 to about 30 carbon atoms.
US20100152200 Alphavirus inhibitors and uses thereof The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of alphaviruses.
CN1634944A Molybdenum, wolfram, molybdenum and wolfram complex, method for making and use in preparing anticancer, antitumor medicament The invention relates to a molybdenum, tungsten and molybdenum-tungsten coordination polymer, preparing process thereof and use thereof in preparation of medicine for prevention and treatment of cancer and tumor. The general formula of the coordination polymer is shown as the formula I or the formula II.
CN1957931A Alkanet for pacifying cheilitis An exterior-applied medicine in the form of ointment or liquid for treating cheilitis and preventing oral lip diseases is proportionally prepared from naphthalene quinone type shikonin, allantoic cord, VE, vaselin, squalane, isooctyl palmitate, beeswax, microcrystalline wax and humectant.
CN103006661A Preparation containing lurasidone hydrochloride and preparation method thereof The invention relates to an oral preparation and a preparation method thereof. The preparation contains lurasidone hydrochloride, a micronized particle of a dispersion supporter, microcrystalline cellulose and a water-soluble polymer adhesive. More specifically, the invention relates to the oral preparation and especially to a tablet. The preparation has a fast dissolution characteristic, and dissolution characteristics of an active component are identical; even though the content of the active component in the preparation changes in a certain range, the dissolution characteristics of the active component are still identical.
WO2013066623A1 Anti Aging Application and Method for Treating Aging There is a topical anti-aging composition which is configured to interfere with the production of tyrosinase, as well as melanin by reacting with melanocytes as well as reacting with, or acting on keratinocytes. The anti-aging composition comprises an emulsion comprising a plurality of active ingredients comprising a plurality of pigmentation reducing elements which are configured to interrupt or prevent the production of tyrosinase and melanin. In addition there are a plurality of antioxidants a plurality of anti wrinkling agents a plurality of anti-inflammatory agents at least one additional agent comprising at least one of an emollient, a proactant and a conditioning agent.
WO2010022634A1 New ethylenediamine derivatives The present invention provides ethylenediamine derivatives of formula (I), its pharmaceutically acceptable salts, its preparation method and uses for the treatment of infectious diseases induced by mycobacterium tuberculosis, especially by multi-drug-resistant mycobacterium tuberculosis. The compound of formula (I) provided by the invention has good extraneous antitubercular activity, and has good internal pharmacokinetic profile.
WO2011052765A1 Alleviator for renal disorders caused by administration of platinum-containing drug Renal disorders caused by the administration of a platinum-containing drug such as cisplatin can be alleviated. In association with the administration of a platinum-containing drug, moisture is loaded by using an infusion solution containing bicarbonate ion such as bicarbonate Ringer's solution.
EP2243483A1 Amlodipine salt compositions for topical application The present application relates to a topical composition comprising one or more amlodipine salts for the treatment of a circulatory condition, such as Raynaud's phenomenon or chilblains. The present application also relates to the use of one or more amlodipine salts to prepare a topical composition for the treatment of a circulatory condition.
US20090018071 Epididymis-specific receptor protein The present invention relates to a novel transmembrane receptor protein which is specific to the mammalian epididymis, DNA sequences which code for the protein and specific ligands and to the use thereof for the preparation of agents for diagnosis of male infertility and for controlling maturation of spermatozoa.
EP2104496A2 Use of nepafenac or derivatives thereof for treating dermatological disorders linked with a keratinisation disorder that may include an inflammatory immuno-allergic component The invention relates to the use of nepafenac or derivatives thereof for producing a pharmaceutical composition for treating dermatological affections linked with a keratinisation disorder that may include an inflammatory immuno-allergic component.
WO2014006250A1 Use of sulphated glycolipids as promoters of neuritic growth and myelination and inhibitors of the proliferation of astroglia and microglia The invention relates to the use of a compound having formula I, in which R1 is an alkenyl group C5-C25 containing one ore more double carbon-carbon bonds, R2 is selected independently from the group consisting of methyl and fluorinated methyl, and R3 and/or R4 is a SO3M group, in which M is selected from the group consisting of hydrogen, alkali metal, ammonium and quaternary amine, the other being hydrogen or acyl, for the production of a drug for the treatment of central nervous system disorders selected from the group consisting of lesions caused by CNS trauma, demyelinating diseases, neuro-inflammatory diseases and mental disorders caused a low level of BDNF. The invention also relates to compounds having formula I, to methods for producing said compounds and to compositions containing same.
CN101429217A Phospholipid type nervonic acid and method for producing the same The invention provides phospholipid nervonic acid, with physical and chemical index in acid value of between 15 and 40mgKOH/g, the content of nervonic acid of between 0.5 and 50 percent by weight, and the content of phosphorus of between 3.0 and 3.8 percent by weight. The invention is to use grease containing the nervonic acid as a raw material to carry out biological enzyme catalyzed ester exchange reaction with phospholipid so as to graft the nervonic acid onto the phospholipid to prepare the phospholipid nervonic acid. The phospholipid nervonic acid has synergistic effect of both the phospholipid and the nervonic acid, and can be absorbed by human body more easily.
WO2012096573A1 Mirna for treating diseases and conditions associated with neo-angiogenesis The invention relates to the diagnostic and therapeutic uses of a miRNA molecule, an equivalent or a source thereof in a disease and condition associated with neo-angiogenesis.
US20110092447 Using inhibitors of histone deacetylases for the suppression therapy of inherited disease predisposing conditions Compounds can be used to act as inhibitors of enzymes having histone deacetylase activity for the medical therapy of conditions which predispose a person for the development of a disease, such as but not limited to cancer, inflammatory or metabolic diseases. Such conditions are linked to genetically inherited mutations of crucial genes which predispose a person with this condition to develop the disease phenotype. Thus, such compounds can be used for a suppressive therapeutic approach—the SUPPRESSION THERAPY—in order to inhibit or delay the onset or progression of the genetically predisposed disorder. Furthermore, a clinically used medicament can be manufactured for the SUPPRESSION THERAPY of such inherited predisposing conditions.
EP2177510A1 Allosteric protein kinase modulators The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
WO2010015212A1 COMPOUND WITH AGITATION EFFECT ON PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR δ, AND PREPARATION METHOD AND USE THEREOF A new compound of formula I with agitation effect on peroxisome proliferator-activated receptor δ (PPARδ), a pharmaceutical composition containing such compound, and the preparation method and the use in the manufacture of a medicament for treating or preventing disease that can be treated or prevented by activating PPARδ thereof, in which the said disease is selected from metabolic syndrome, obesity, lipid abnormality, pathoglycemia, insulin resistance, senile dementia and tumor. A new intermediate used in the preparation of said new compound and the preparation method thereof.
CN103006578A Application of salvianolic acid A lyophilized powder injection in preparation of drugs for improving neurological function symptoms after cerebral ischemia The invention relates to application of salvianolic acid A lyophilized powder injection in preparation of drugs for improving neurological function symptoms after cerebral ischemia. The salvianolic acid A lyophilized powder injection comprises, by weight, 20-60g of salvianolic acid A, 20-60g of filling agent, and an antioxidant accounting for 0.02%-0.1% of the total amount of the finished product.
WO2013107743A1 Spiroindoline derivatives as gonadotropin- releasing hormone receptor antagonists Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selded from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reprodudive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
US20100331277 Antimicrobial locking solutions comprising taurinamide derivatives and biologically acceptable salts and acids, with the addition of small concentrations of heparin The present invention relates to inhibiting or preventing infection and protecting against patency complications after a blood catheter has been inserted in a patient comprising administering to the device a pharmaceutically effective amount of a composition comprising: (A) at least one taurinamide derivative, (B) at least one compound selected from the group consisting of biologically acceptable acids and biologically acceptable salts thereof; and (C) heparin at a low concentration.
CN101041656A Fluorine carbostyrile-oxazolidinone derivative and composition thereof, preparation method and usage The invention discloses a making method and application of fluocarbostyrile-oxazolidinone derivant with structural general formula as formula I, wherein R1 is C1-C4 alkyl, C3-C6 cycloalkyl or C1-C4 halogenated alkyl groups; R2 is H or C1-C4 alkyl; R3 is H, halogen or C1-C4 alkoxy; or R2 and R1 forms bridge as formula II; X is S, O or CH2; or R3 and R1 forms bridge as formula III; Z is S, O or CH2; R4 is H or C1-C4 alkyl; R0 is H or halogen; the derivant possesses excellent antibacterial activity, which can be applied widely.
CN102872015A Stephanotis total alkaloid extract as well as preparation method and application thereof The invention discloses a stephanotis total alkaloid extract as well as a preparation method of the stephanotis total alkaloid extract. The preparation method of the stephanotis total alkaloid extract comprises the following steps of: grinding the dried stephanotis, heating and extracting, and decompressing and condensing the filtrate; diluting with heating water, and acidifying and filtrating to obtain a filtrate; alkalifying and filtrating to obtain the filtrate, and performing molecular weight cut off filtration on the obtained filtrate through a ceramic membrane filter; extracting with n-butyl alcohol, decompressing and condensing; spray drying the concentrated solution to obtain a dried powder extract; adding ethanol for ultrasonic extraction, mixing the extracting solution, absorbing the extracting solution by a sephadex column, eluting with 90% to 95% of ethanol, segmentally collecting, identifying through a high performance thin layer chromatography, mixing the parts containing alkaloids, freezing at a low temperature, and separating out an alkaloid crystal crude product; and adding ethanol for dissolving, standing and freezing to obtain a stephanotis total alkaloid pure product. A stephanotis total alkaloid medicinal preparation provided by the invention has the effect of adjuvant therapy on leucopenia, in particular to leucopenia of the tumor patients caused by radiotherapy and radiotherapy, and the leucopenia caused by other medicines.
CN102430020A Process method for leading easily-layered paste material to be uniform in production of compound south-star pain relieving paste The invention discloses a process method for leading an easily-layered paste material to be uniform in production of compound south-star pain relieving paste. The process method comprises the following steps of: (1) heating a base material and auxiliary materials of the paste, adding fine medicine powder after melting, stirring and obtaining the uniform paste material; (2) distributing the paste material into a plurality of shallow pans uniformly; (3) rapidly reducing the temperature, reducing the sedimentation velocity of the medicine powder and leading the medicine powder to be solidified; (4) dividing the solidified paste material; dividing the paste material in each shallow pan according to the same specifications and the same shapes into a plurality of stripy blocks; (5) numbering all the divided stripy blocks of the paste material in each shallow pan respectively according to the same numbering mode; (6) putting the stripy blocks of the paste material with same number in all the shallow pans together, and respectively grouping; and (7) respectively stirring the paste material in each group by a stirring machine, leading the paste material to be uniformly mixed by a medicine film machine for production of next procedure. In the process method, the layering problem of the paste material is thoroughly solved, the paste material with all the uniform components is obtained, and the difficulty which can not be solved for long time in production of the field is solved.
US20080181894 Tumor/cancer antigens; solid phase synthesis; drug screening The present invention relates to methods using newly identified cancer related polynucleotides and the polypeptides encoded by these polynucleotides. The invention further relates to the use of such “cancer antigens” for diagnosing cancer and cancer metastases. The invention relates to the use of these cancer antigens employing expression vectors, host cells, antibodies directed to such cancer antigens, and recombinant methods and synthetic methods for producing the same. Also provided are diagnostic and prognostic methods for detecting, treating, or preventing cancer, for suppressing tumor progression and minimal residual tumor disease, and therapeutic methods for treating such disorders. The invention further relates to screening methods for identifying agonists and antagonists of the cancer antigens of the invention. The present invention further relates to inhibiting the production and function of the polynucleotides and polypeptides of the present invention.
CN1833639A 'Xindakang' dispersion tablets and prepn. method A dispersing tablet of Xindakang with high solubility and disintegrating speed for treating ischemic heart disease, arrhythmia, hypertension, hyperlipemia, hyperviscosity blood, etc is prepared from flavone acetylsalicylate and proper additive. Its preparing process is also disclosed.
WO2008049856A3 Methods of treating pain using cdk inhibitors The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases.
US8450306 Bradykinin B1-receptor antagonists Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumor pain and headache diseases. The following is exemplary:
EP1939173A1 O-substituted-dibenzyl urea- or thiourea- derivatives as trpv1 receptor antagonists The invention relates to compounds of formula (I) wherein R is halogen; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, aminomethyl, 2-aminoethyl, 3-aminopropyl, 3-amino-2-hydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxypropen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, 4-hydroxybenzyl, and 4-aminobenzyl; R2 is O or S; R3 is tert-butyl or trifluoromethyl; n is an integer selected from 0, 1 or 2. The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, haemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.
WO2012035131A1 Treatment of abl overexpressing b-cell lymphoma The invention relates to bcr-abl inhibitors, such as imatinib, dasatinib or nilotinib, for use in the treatment of ABL overexpressing B-cell lymphoma, in particular mucosa-associated lymphoid tissue (MALT) lymphoma, and to compositions further comprising an antibiotic and/or proton-pump inhibitor for such use. Likewise it relates to bcr-abl inhibitors for use in the preparation of a medicament for the treatment ABL overexpressing B-cell lymphoma, and to a method of treatment of ABL overexpressing B-cell lymphoma comprising administering a bcr-abl inhibitor. These claims are based on the observation that ABL1 plays an important oncogenic role in the pathogenesis of MALT lymphoma.
US7795301 preventing myxoviruses infection using 3-(acetylamino)-2-{3-(acetylamino)-4-{[amino(imino)methyl]amino}-6-carboxy-3,4-dihydro-2H-pyran-2-yl)-1-[1,2-dihydroxyethyl]-19,20-dihydroxy-3,16-dioxo-2,17-dioxa-4,15-diazaicos-1-yl}-4-{[amino(imino)methyl]-amino}-3,4-dihydro-2H--pyran-6-carboxylic acid; viricides The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; and n is an integer from 10 to 18 or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection.
CN1839844A Gancilorvir eye ointment and its preparation The invention relates to an antiviral Ganciclovir eye ointment comprising medicinal adjuvant and antiviral effective amount of Ganciclovir dispersed in the adjuvant, the content of Ganciclovir being 0.5-3.0 wt%, its preparing process consist of grinding Ganciclovir, sieving, heating the adjuvant and filtering, heating to 130-150 deg C, sterilizing 60-80 minutes, cooling down to room temperature, moistening the Ganciclovir with sterilization liquid wax, charging bactericidal agent and homogenizing, finally loading into eye ointment.
WO2012115176A1 3-(biaryloxy)propionic acid derivative The present invention provides a compound which has excellent anti-platelet aggregation activity and is useful for prophylaxis and/or treatment of thromboembolic diseases. A compound represented by general formula (I) or a pharmacologically acceptable salt thereof. (In general formula (I), R1 represents a halogen atom, a cyano group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group; R2 represents a hydrogen atom, a halogen atom, a cyano group or a C1-4 alkyl group; R3 represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, a C1-4 alkyl group or an amino group; R4, R5 and R6 each represents a hydrogen atom, a halogen atom or a C1-4 alkyl group; R7 and R8 each represents a hydrogen atom or a C1-4 alkyl group; R9 and R10 each represents a hydrogen atom, a C1-4 alkyl group or a group that forms a C3-5 cycloalkyl group; X1-X2 represents -C(Ra)(Rb)-C(=O)-, -N(Rc)-C(=O)-, -CH=CH-, -CH=C(Rd)-C(=O)-, -N=CH-, -CH2-O-C(=O)-, -CH2-N(Re)-C(=O)- or -CH2CH2CH2-; Y represents a nitrogen atom or =C(Rf)-; Z represents a nitrogen atom or =CH-; Ra, Rb, Rc, Rd and Re each represents a hydrogen atom or a C1-4 alkyl group; and Rf represents a hydrogen atom, a halogen atom or a C1-4 alkyl group.)
CN101428037B Anti-apolexis composition containing repair factor The invention discloses antiaging composition which contains repair factors and can realize synergism to the body on multiple layers and in multiple sites. The composition comprises vitamin c, oligomeric proantho cyanidins, gadol glycoside, vitamin B6, vitamin B1, vitamin B2, nicotinic acid, taurine, arginine, lysine, inositol and zinc salt. The components of the composition are integrated all sidedly with key points and pertinency according to the physiological characteristic of human body, the recombined repair factors can better exert the synergistic effect, completely repair the activity of cells, tissues and organs of the human body, and inhibit bio-garbage generated by metabolism, thereby improving the aging symptom of the human body and preventing sub-health.
US20120329840 Novel modulators of sphingosine phosphate receptors Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.
US8481572 Pharmaceutical compositions and methods for the treatment of cancer Provided is a pharmaceutical composition including as an active component a compound of formula (I): wherein X and (R1)n are as defined, and a physiological acceptable carrier. Also provided is a method for treating cancer including administering to an individual in need of such treatment an effective amount of the presently described pharmaceutical composition.
CN101773505A Cefpiramide-containing medicine used for injection The invention relates to a cefpiramide-containing medicine used for injection, which is used for an injection used for treating diseases. The invention discloses the medicine used for the injection, which comprises a component A of cefpiramide and a component B of a solvent which contains organic base and is exclusively used for the cefpiramide used for the injection, wherein the cefpiramide and the solvent are separately packaged, and the weight ratio of the component A to the component B is 1:5 to 20. The invention is easy to dissolve, is simple and convenient to operate and is safe during injection.
CA2430897C Liposomal composition comprising water-soluble corticosteroids for the treatment of inflammatory disorders A pharmaceutical composition for parenteral administration, comprising liposomes composed of non-charged vesicle-forming lipids, including up to 20 mole percent of an amphipathic vesicle-forming lipid derivatised with polyethyleneglycol, and optionally including not more than 10 mole percent of negatively charged vesicle-forming lipids, the liposomes having a selected mean particle diameter in the size range between about 40-200 nm and containing a water soluble corticosteroid for the site-specific treatment of inflammatory disorders, is provided.
US20080096828 7-Quinolyl ketolide antibacterial agents 15-fluoroketolides of the formula having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections.
WO2009097490A1 1H-PYRAZOLO[3,4-D]PYRIMIDINE, PURINE, 7H-PURIN-8(9H)-ONE, 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE, AND THIENO[3,2-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES The invention relates to 1H-pyrazolo[3,4-d]pyrimidine, purine, 7H-purin-8(9H)-one, 3H-[1,2,3]triazolo[4,5-d]pyrimidine, and thieno[3,2-d]pyrimidine compounds, compositions comprising the compounds, and methods for making and using the compounds.
WO2010149943A1 New compounds and medical use There is provided compounds of formula (I), wherein the wedged bonds, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, X and Y have meanings given in the description, and pharmaceutically- acceptable salts thereof, which compounds are useful in the treatment of cancer and conditions affected by inhibition of angiogenesis.
US20080187605 Preventing pathological nerve cell suicide (neuroapoptosis) in immature nervous systems By disrupting a natural process used by developing mammalian brains to prune and delete surplus neurons, surgical anesthetics and other drugs that suppress brain activity in fetuses and infants can trigger permanent pathological brain damage. That type of damage can be prevented by drug interventions that block one or more “upstream” events that otherwise would lead to the release of “Cytochrome C”, a messenger molecule that triggers apoptosis (programmed cell death) among immature neurons. Lithium is a potent protective agent that can be coadministered along with ketamine or other NMDA-acting or GABA-acting anesthetics and anticonvulsants. Xenon gas triggers only mild damage, and can enable improved anesthesia when combined with other drugs. Other protective drugs (also called safener drugs), and treatments that can prevent or minimize fetal alcohol syndrome, also are disclosed.
US20110201690 Deuterium-enriched dapoxetine The present application describes deuterium-enriched dapoxetine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20110021447 Acne treatment composition and methods for using An acne treatment composition is provided according to the present invention. The acne treatment composition includes an effective amount of an anti-acne component to provide anti-acne properties to skin tissue, an effective amount of a skin bounding polymer component to provide sustained release of the anti-acne component over a prolonged period of time after application of the acne treatment composition to skin tissue, and water. A method of using an acne treatment composition is provided.
US7189537 Comprises oncogenic nucleotide sequences for use in diagnosis, prevention and treatment of various cancers; gene therapy and antisense agents A human protooncogene having a base sequence of SEQ ID: 1 or a fragment thereof is overexpressed in various cancer tissues and can be used in diagnosing various cancers and an antisense gene complementary thereto can be used in treating cancers.
WO2013184681A1 Crystalline forms of an androgen receptor modulator Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
CN102485217A Letrozole tablet with high dissolubility and preparation method thereof The invention discloses a Letrozole tablet with high dissolubility and a preparation method thereof. An effective component of the tablet is Letrozole, and polyvinylpyrrolidone K30, tween 80, mannitol, lactose, microcrystalline cellulose, cross-linked polyvinylpolypyrrolidone and magnesium stearate are used as accessories. The product of the tablet has stable quality and high dissolubility, enables absorption of Letrozole in a human body to be increased and bioavailability to be effectively improved and is easy to prepare and applicable to industrial production.
WO2014091430A1 Pharmaceutical composition comprising a meglitinide and a thiazolidinedione, and use thereof The invention relates to an oral pharmaceutical composition combining a thiazolidinedione salt and a meglitinide and/or the pharmaceutically acceptable salts thereof, as well as pharmaceutically acceptable vehicles and/or excipients, with improved release of hypoglycemic agents. The invention also relates to the use of said composition having synergic therapeutic activity and indicated for the treatment of hypoglycemia and for the control of glycemic levels and associated comorbidities.
CN1973841A Liniment for treating parotitis The present invention discloses one kind of liniment for treating parotitis, and aims at providing one kind of externally applied parotitis treating medicine with fast acting, obvious pain relieving effect, short treating period and convenient use. The liniment for treating parotitis is compounded with moroxydine in 0.5-10 weight portions and vinegar in 25-50 weight portions, and through grinding moroxydine into powder and mixing with vinegar.
WO2010013086A1 Phosphorylated dendrimers as antiinflammatory drugs Dendrimers with monophosphonic or bisphosphonic terminations for the treatment of inflammatory diseases.
CN103446181A Preparation process of peritoneal dialysate with physiologic pH value The invention provides a preparation process of peritoneal dialysate with a physiologic pH value. The process comprises raw material proportioning and a preparation process. The process is characterized in that the preparation process comprises the following steps: adding fresh water for injection into a proportioning container; inputting glucose, sodium chloride, calcium chloride, and magnesium chloride in prescription amount; after stirring and dissolving, adding water for injection to full dose to prepare a liquid A; adding fresh water for injection into another proportioning container; inputting sodium lactate; after stirring and dissolving, adding water for injection to full dose to prepare a liquid B; after uniformly stirring; respectively adding a pH adjustor into the liquid A and the liquid B to adjust the liquid medicine to appropriate pH values; after pre-filtering and terminal-filtering, respectively filling the liquid A and the liquid B to two chambers of a double-chamber transfusion bag in volume ratio of 1:1; plugging; sterilizing by water bath; sterilizing to obtain the peritoneal dialysate with low glucose degradation products and the physiologic pH value, wherein the pH value of the mixture of the liquid A and the liquid B reaches 6.8-7.4.
CN103156862A Compound voriconazole eardrops and preparation method thereof The invention relates to eardrops, and in particular relates to compound voriconazole eardrops and a preparation method thereof. The compound voriconazole eardrops is characterized in that 0.1-2.0g of voriconazole, 0.1-3.0g of hydrocortisone, 5-40g of hydroxypropyl-beta-cyclodextrin, 10-80ml of polyethylene glycol, 0.1-3.0g of menthol, 0.1-2.0g of sodium chloride, 0.01-0.1g of ethylparaben, 5-60g of glycerin and 10-100ml of ethanol are contained in per 100-1000ml of the eardrops. The compound voriconazole eardrops disclosed by the invention has the beneficial effects that the composing prescription is reasonable and scientific and the voriconazole with the broadest antifungal spectrum is selected as the main medicine, so that the eardrops has antibacterial activity on all candida; the toxic and side effects of systemic administration can be reduced through local application and in the meantime, the eardrops is convenient for application, capable of increasing the curative effect and low in price when being directly used as the eardrops; and the eardrops is stable in quality and little in irritation and adverse reaction.
WO2012135465A3 Treatment of glaucoma A method is provided for treating patients suffering from elevated intraocular pressure or fluctuation in intraocular pressure, including for example glaucoma patients. The method comprises administered to the patient an inhibitor of orexin activity in an amount sufficient to reduce intraocular pressure or intraocular pressure fluctuation in one or both eyes of the patient.
WO2005106459A1 Method of determining ability of drug to bind to troponin i and test drug for the determination A method of screening a therapeutic drug for cardiac failure attributed to dilation failure, intended to facilitate the discovery of a drug for improving myocardial relaxation as a specific medicine, namely, a therapeutic drug for cardiac failure attributed to dilation failure. Also, there is provided a screening reagent therefor. In particular, there is provided a method of assaying the activity of drug on binding between actin/tropomyosin complex and troponin I, characterized in that the method comprises adding a test drug to an aqueous solution containing troponin I, troponin C, actin, tropomyosin and ATP; effecting reaction of the mixture; fractionating any precipitate from the reaction mixture; conducting separation of any precipitate lying in a liquid having any supernatant removed therefrom by polyacrylamide electrophoresis; staining separation bands with a colorant; and measuring the amount of separated matter in the separation band of troponin I.
CN101584705B Medicament composition for treating diabetes and complications of diabetes The invention provides an oral medicament composition for treating diabetes and the complications of diabetes, belonging to the field of medicines. The oral medicament composition for treating diabetes and the complications of diabetes comprises migltol and heparin or low molecular heparin or a medicinal salt of the heparin or the low molecular heparin in the weight ratio of 1:0.1-9. The medicament composition plays a good synergic action on lowering blood sugar, can reduce the complications of diabetes and generate positive effect on the prognosis of a diabetic who takes the oral medicament composition for a long time so that the oral medicament composition for treating diabetes and the complications of diabetes is quite beneficial to the recovery of the diabetic.
US20120308525 Nutritional compositions including a high protein component and exogenous nucleotides Nutritional compositions and methods of making and using the nutritional compositions are provided. In a general embodiment, the present disclosure provides a nutritional composition including a high protein component and one or more exogenous nucleotides. The nutritional compositions can be specifically used to accelerate and improve wound healing in a mammal.
WO2009106586A1 Quinolines as inhibitors of farnesyl pyrophosphate synthase The invention relates to a compound of formula (I) wherein the substituents are as described in the specification, which are useful as farnesyl pyrophosphate synthase modulators, e.g. in the treatment of proliferative diseases, to methods of manufacturing such compounds and to intermediates thereof.
CN103751206A Medicinal composition for preventing Alzheimer's disease and application thereof The invention belongs to the technical field of medicine, particularly relates to a medicinal composition for preventing Alzheimer's disease and application thereof. The medicinal composition is prepared from the following raw materials: friedelin-3beta-ol, resveratrol, Astragalus polysaccharide component A1, Astragalus polysaccharide component A2 and Lycium barbarum polysaccharide component I. The medicinal composition provided by the invention has distinct effect of preventing Alzheimer's disease, has the advantages of stable quality control and no toxicity, and is suitable for long-term administration.
US20090005328 Methods of modulating tubulin deacetylast activity The present invention provides methods for identifying agents that modulate a level or an activity of tubulin deacetylase polypeptide, as well as agents identified by the methods. The invention further provides methods of modulating tubulin deacetylase activity in a cell. The invention further provides methods of modulating cellular proliferation by modulating the activity of tubulin deacetylase.
WO2008144423A3 Compositions comprising a gpr109 ligand for treating disorders of the digestive tract and/or cancer Pharmaceutical compositions containing an effective amount of a ligand for GPR109 to decrease intracellular cAMP levels of a subject in combination with an effective amount of a DNA methyl transferase inhibito to reduce or inhibit downregulation of GPR109 in the intestinal epithelial cells of the subject relative to a control are provided. It has been discovered that ligands for GPR109 can be used to treat one or more symptoms of cancer, inflammatory disorders, and diarrhea. Representative CPR109 ligands include, but are not limited to butyrate, β-hydroxybutyrate, nicotinic acid, acifran, and octanoate. Suitable DNA methyl transferase inhibitors include 5-azacytidine, 5-aza-2'-deoxytidine, 1-β-D-arabinfαrnosyl-5- azacytosine and dihydro-5-azacytidine. Typically, the compositions are formulated to achieve a GPR109 ligand serum blood level of about 1 to about 1000 μM. The compositions are useful for the treatment of one or more symptoms of cancer. Preferred cancers that can be treated using the disclosed compositions include, but are not limited to colon cancer, breast cancer and leukemia. Methods for treating cancer, inflammatory disorders, and diarrhea are also provided.
EP2305680A2 Novel salts of (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol The present invention relates to novel salts of (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1 -methanol of Formula I or solvates or hydrates thereof, wherein M represents hemimalonate, malonate, hemioxalate, oxalate, hydrobromide, dihydrobromide, hemimaleate, maleate.
WO2014114532A1 Fluoro-[1,3]oxazines as bace1 inhibitors The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
CN103202817A Preparation method for mannitol grains capable of being directly pressed The invention discloses a preparation method for mannitol grains capable of being directly pressed. The preparation method is characterized by comprising the following steps of: taking mannitol, crushing and passing through a 80-mesh sieve, so as to obtain a mannitol powder; and performing top-jet granulation on the mannitol powder by virtue of a fluidized bed, by using adhesive aqueous solution as top-jet slurry, granulating and then sieving, so as to obtain the mannitol grains capable of being directly pressed. The preparation method disclosed by the invention is simple in granulation process and saving in labour; a mixed adhesive is preferentially chosen; and the obtained grains are capable of meeting requirements in the aspects of brittleness, uniformity and hardness, better in uniformity, flowability and dispersity, and more convenient to package and transport.
CN101336955A Gynostemma pentaphylla extract and preparation method thereof and use thereof in preparing medicine for preventing and treating fatty liver and sub-health The invention discloses a Gynostemma pentaphyllum extract containing Gynostemma pentaphyllum polysaccharides and Gynostemma pentaphyllum total saponins at a weight ratio of 1:(1-5). The invention also discloses an application thereof in preparing medicaments for preventing and treating fatty liver and sub-health, and a preparation method thereof. The Gynostemma pentaphyllum extract has good effects of preventing and treating fatty liver and sub-health.
WO2009025919A3 5-propargyl-pyrimidine derivatives as inhibitors of dihydrofolate reductase with antibacterial antiprotozoal, antifungal and anticancer properties The compositions and methods described herein discloses the design, synthesis and testing of compounds of formulae I or Ia that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2, 4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin- resistant Staphylococcus aureus, fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii. These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti- cancer therapeutics.
EP2468762A1 Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size The present invention relates to a pure polymorph of Nor-UDCA or Bis-nor-UDCA, or of a pharmaceutically acceptable salt thereof. The invention further provides a pharmaceutical composition comprising the polymorph of the invention, and a method for preparing the polymorph. The invention includes the pharmaceutical use of the polymorph or of the pharmaceutical composition of the invention.
US20110039933 S1p-1 receptor agonists The invention provides compounds formula (I), their preparation, and their use as pharmaceutically active immuno-suppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.
US7105162 Peptide or protein from a pathogenic or tumor agent having immunomodulatory activity with an adjuvant capable of increasing the binding of the peptide to the cells of the individual or increasing the entry of the peptide into the cells; strengthening immunomodulatory activity; polyamino acids adjuvants Pharmaceutical composition containing at least one peptide or protein (fragment) with an immunomodulatory activity together with an adjuvant. The peptide is derived from a pathogenic agent or a tumour antigen. The adjuvant is capable of increasing the binding of the peptide to the cells of the individual to be treated or of increasing the entry of the peptide into the cells and strengthening the immunomodulatory activity of the peptide. Preferred adjuvants are basic polyamino acids such as polyarginine or polylysine, optionally conjugated with a cellular ligand such as a carbohydrate group or transferrin. The composition is particularly intended for use as a vaccine, e.g. as a tumour vaccine.
US20110172305 Endocannabinoids for Enhancing Growth and Development in Infants The present invention relates to a method for promoting infant feeding, growth or development comprising administering to an infant a formula or a pharmaceutical composition comprising an endocannabinoid in an amount sufficient to promote feeding, growth or development. The present invention also relates to an infant formula comprising an enhanced amount of an endocannabinoid. The infant formula of the invention may be in a powder form or in a liquid form. The infant formula or the pharmaceutical composition may further comprise an endocannabinoid-promoting compound.
US6861059 Administering DP-107 or a pharmaceutically acceptable derivative thereof along with at least one therapeutic agent; synergistic Novel antiviral combinations for the treatment or prevention of viral infections, in particular, HIV, are disclosed. This new antiviral therapy employs either DP-178 or DP-107, viral fusion inhibitors, in combination with at least one other antiviral therapeutic agent. The combinations of the invention are better than single therapies alone, and in certain cases are synergistic. The use of DP-178 or DP-107 is an ideal therapy to combine with another antiviral, given both the novel mechanism which this therapeutic blocks HIV transmission and the non-toxicity of the therapeutic.
CN103565828A Chlorine dioxide gel and manufacturing method thereof A method for manufacturing chlorine dioxide gel includes the following steps: a step of dissolving peg-copolymer bis-decyltetradeceth in hot water to form an aqueous solution of peg-copolymer bis-decyltetradeceth; a step of heating the aqueous solution of peg-copolymer bis-decyltetradeceth obtained in the above step to form a gel like colloid; a step of dissolving pure chlorine dioxide gas in water to form an aqueous solution of chlorine dioxide; and a step of uniformly mixing the aqueous solution of chlorine dioxide and the colloid of peg-copolymer bis-decyltetradeceth to form a chlorine dioxide gel, whereby with the above steps, a method for manufacturing chlorine dioxide gel that stably preserves chlorine dioxide gas in a gel is provided.
US6919377 Cyclohexylamine derivative as subtype selective NMDA receptor antagonists Described are compounds of Formula I and Formula II and their pharmaceutically acceptable salts. The compounds of Formulas I and II are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.
WO2008018448A1 Activator comprising biosurfactant as the active ingredient, mannosyl erythritol lipid and method of producing the same At least one kind of a biosurfactant, in particular, a mannosyl alditol lipid (MEL, MML or the like) or a triacyl derivative of the same is used as an active ingredient. Thus, it becomes possible to provide an activator or an anti-aging agent that is excellent in a cell activating effect and an anti-aging effect and has such a high safety as withstanding to prolonged use. Also, cosmetics, quasi drugs, drugs, foods and drinks containing the same as the active ingredient are provided. Moreover, an MEL wherein the mannosyl erythritol skeleton in its molecular structure is 1-O-β-D-mannopyrasyl-meso-erythritol and a method of microbiologically producing the same are provided.
EP1918278A1 Sulfonylamino derivatives which inhibit matrix-degrading metalloproteinases Compounds of formula I wherein: W is -OH or -NHOH; X is an optionally substituted heterocycle, -NR1SO2R2, heterocyclylalkylthio; -CONR2R3, or-NR1COR2, Y, Z, R1-R3 and n are as defined in the application. Compounds (I) are inhibitors of matrix-degrading metalloproteinases and are useful for the treatment of related conditions.
CN101683532A Ophthalmic compound medicinal preparation containing hyaluronic acid or sodium hyaluronate The invention relates to an ophthalmic compound medicinal preparation containing hyaluronic acid or sodium hyaluronate, which is characterized in that the preparation comprises macrolide antimicrobialdrugs and steroidal anti-inflammatory drugs, can be antimicrobial and anti-inflammatory and obviously improves the treatment effects of ophthalmic infection and inflammation. The preparation takes the hyaluronic acid and sodium hyaluronate as carries, not only lengthens the residence time of medicines on the eyes so as to improve the bioavailability, but also lightens the irritation of the medicines to the eyes and improves the comfort after administration.
CN101850042A Medicament for treating fractures The invention discloses a medicament for treating fractures, which is prepared from the following medicaments in percentage by weight: calcined pyrite, ground beetle, frankincense, myrrh, dragon's blood, raw pinellia tuber, crabshell and catechu. The formula has rigorous compatibility; the calcined pyrite serving as a monarch medicament in a prescription is used for bonesetting and analgesic therapy, and is the key medicament of the bonesetting of orthopedics; the ground beetle is used for the reunion of fractured tendons and bones and is used as a ministerial medicament; the frankincense, the myrrh, the dragon's blood and the catechu are used for promoting blood circulation by removing blood stasis, promoting tissue regeneration and growing the tendons and stopping bleeding and removing swelling, and are used as adjuvant medicaments together; and the pinellia tuber and the crabshell are used for detoxifying and lowering adverse-rising qi, and are used as historical medicaments together. The medicaments have the effects of promoting blood circulation by removing blood stasis and growing the tendons and setting the bones. The medicament of the invention makes osteotylus form quickly, has the good treatment effect, simplified medicinal odors and low cost, solves the problems of various medicinal odors, high cost, serious gastrointestinal reactions and the like in the process of treating fractures and traumatic injury currently, and overcomes the defects of treating the fractures by using a mechanical method in western medicine. The clinical healing can be achieved after one month of the fracture, and the fracture can be healed totally for 2 to 3 months. The medicament has simplified medication and low cost, and is accepted by bone fracture patients in each level.
US7462614 7-(2-Bromophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine; to treat neoplasms; polo like kinases inhibitors; antineoplastic/antiproliferative agents; cyclization of 1,2,4-triazine derivatives; coupling if imidazo[5,1-f][1,2,4]triazines with amine or halogen derivatives The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
US20120150096 Implantable or insertable medical devices for controlled drug delivery Implantable or insertable medical devices are provided, which comprises: (a) a biocompatible polymer; and (b) at least one therapeutic agent selected from an anti-inflammatory agent, an analgesic agent, an anesthetic agent, and an antispasmodic agent. The medical devices are adapted for implantation or insertion at a site associated with pain or discomfort upon implantation or insertion. In many embodiments, the therapeutic will be selected from at least one of (i) ketorolac and pharmaceutically acceptable salts thereof (e.g., ketorolac tromethamine) and (ii) 4-diethylamino-2-butynylphenylcyclohexyl glycolate and pharmaceutically acceptable salts thereof (e.g., oxybutynin chloride). Also provided are uses for the implantable or insertable medical devices, which uses comprise reducing pain or discomfort accompanying the implantation or insertion of such devices. Further uses may comprise reducing microbial buildup along the device. Methods for manufacturing implantable or insertable medical devices are also provided.
WO2009093981A1 Triazine compounds as kinase inhibitors The present invention relates to triazine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to morpholino substituted triazines, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with mTOR kinases or PI3 kinases. The compounds are of the formula (I).
WO2006088705A1 Terphenyl guanidines as [beta symbol] -secretase inhibitors The present invention provides terphenyl guanidine compounds of formula I. The present invention also provides methods for the use thereof to inhibit ß-secretase (BACE) and treat ß-amyloid deposits and neurofibrillary tangles.
WO2010008777A3 Fused azabicyclic pyridines Azabicyclic pyridine derivatives and pharmaceutically acceptable salts thereof are disclosed herein These compounds are useful as EP2 antagonists. Uses of these compounds and pharmaceutical compositions thereof are also disclosed.
WO2014068171A1 N-substituted 4-aminophenols and corresponding quinone imines Compounds of formula I or formula II, wherein Q1Q3 and R1-R5 are as defined in the claims, exhibit CytC derived peroxidase inhibiting activity and are thus useful as CytC derived peroxidase inhibiting agents.
EP2112167A2 Humanized ANTI-ERBB2 antibodies and treatment with ANTI-ERBB2 antibodies The present application describes humanized anti-ErbB2 antibodies and methods for treating cancer with anti-ErbB2 antibodies, such as humanized anti-ErbB2 antibodies.
US20080241249 Cyanoacrylate composite An adhesive composite composition is provided including one or more polymerizable monomers and one or more metal stearates. The one or more polymerizable monomers may be a cyanoacrylate monomer. The adhesive composite composition may further comprise a plasticizer, an initiator, a rate modifier, a stabilizer, a colorant, a heat dissipating agent, or other additives. Methods for the application of the adhesive composite compositions to living tissue are also provided. The adhesive composite composition provides an adhesive composite material upon polymerization which is a polymer matrix entrapping the metal stearate. Polymerization of the adhesive composite composition at a site on living tissue provides an adhesive composite material which promotes microcirculation and tissue growth at the site of application of the adhesive composite composition.
CN103405470A Application of hyaluronic acid and hyaluronate in preparation of composition for treating and alleviating xerostomia The invention provides an application of hyaluronic acid and hyaluronate in preparation of a composition for treating and alleviating xerostomia and the composition for treating and alleviating xerostomia. As hyaluronic acid and hyaluronate thereof are in double helix columnar structures, and massive hydroxyls exist inside the double helix structures, the hyaluronic acid and hyaluronate thereof have a very good water holding effect, so that the hyaluronic acid and hyaluronate thereof have lasting moisturizing effect on oral cavity. Furthermore, the hyaluronic acid and hyaluronate thereof can promote wound healing and have the effects of healing anabrosis and the like. In addition, the hyaluronic acid and hyaluronate thereof are colorless and tasteless and free from toxicity, belong to synthetic substances in human body, and are easy to be compatible with ions such as sodium, potassium, calcium, zinc, ferrum and silver ions, so that the hyaluronic acid and hyaluronate thereof have the taste which is suitable for being accepted by human body.
CN103145674A Crystal forms of 7-hydroxyl isoflavone, preparation methods thereof, pharmaceutical composition of methods and purpose The invention discloses five crystal forms of 7-hydroxyl isoflavone, preparation methods thereof, pharmaceutical composition of the methods and a purpose, and particularly relates to five forms including a crystal form A, a crystal form B, a crystal from C, a crystal form D and a crystal form E, wherein the crystal form A, the crystal form B, the crystal form C, the crystal form D and the crystal form E exist under the solid state of a 7-hydroxyl isoflavone compound. The invention particularly relates to the preparation methods of samples of the five crystal forms. The invention further relates to various preparations and the pharmaceutical composition. The various preparations and the pharmaceutical composition are prepared and developed from materials of different crystal forms of the 7-hydroxyl isoflavone, and the materials of the different crystal forms serve as active ingredients. The various preparations and the pharmaceutical composition play a good clinical treatment function on preventing and curing cardiovascular and cerebrovascular diseases, a brittle-bone disease, inflammation, metabolic diseases and other diseases. The crystal forms can affect absorption speed of effective ingredients of the solid medicine in a living body, strengthen or reduce blood concentration in the living body, and accordingly the treatment function of the medicine on a clinic is affected.
US20100015255 Compositions and methods for treating hypercholesterolemia using ortanique peel extract The invention relates to compositions and methods for treating hypercholesterolemia, including methods for increasing HDL cholesterol levels, using a composition comprising an extract from the Ortanique peel. The invention also relates to compositions and methods for treating hypercholesterolemia, including methods for increasing HDL cholesterol levels, using a composition comprising substantially similar amounts of tetramethylscutellarein and nobiletin by weight and/or a composition comprising substantially similar amounts of tetramethylscutellarein, nobiletin, and tangeretin by weight.
CN103356625A Use of pyrazolopyrimidine compound in treatment on candida parapsilosis infected diseases The invention discloses a use of a pyrazolopyrimidine compound in treatment on candida parapsilosis infected diseases. The pyrazolopyrimidine compound is N3-(4-fluoropentyl)-1H-pyrazolo[3,4-D]pyrimidine-3,4-diamine.
US7325355 Methods for treatment of atherosclerosis using 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindoline Methods and compositions for the prevention and treatment of all forms of atherosclerosis are described. Administration of compounds such as thalidomide, its analogs, hydrolysis products, metabolites, derivatives and precursors as well as additional compounds capable of inhibiting tumor necrosis factor α(TNF-α) are used in the invention. Also disclosed is the coating of prosthetic devices, such as stents, with the compounds of the invention for the prevention and/or treatment of restenosis.
US20100311682 Antimelancholic medicine prepared with jujube camp materials The antimelancholic medicine or health products prepared with jujuba cAMP materials and the preparative method are provided in the present invention.
CN101919844A Compound for controlling autoimmune disease and use thereof The invention relates to a compound for controlling autoimmune disease and use thereof, wherein, the compound comprises berberine and pharmaceutically acceptable salt or a derivative thereof, and the autoimmune disease refers to type I diabetes or insulitis and the like. The invention further provides the new use of the berberine for the first time; and the berberine has strong pharmacological effects, no toxic side effects and good pharmaceutical prospect.
WO2012110440A9 6 - cyclobutyl - 1, 5 - dihydro - pyrazolo [3, 4-d] pyrimidin- 4 - one derivatives their use as pde9a inhibitors The invention relates to novel pyrazolopyrimidinones according to formula (I), wherein R1 is a pyridyl or pyrimidinyl group and D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3-or 4-pyridyl. The new compounds are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.
CN101125142A Application of artemisine in preparing artitumor multi-medicine-resistant medicine The present invention discloses an application of artemisinin, dihydroartemisinin and artesunate in the preparation of anti-tumor multi-drug resistant drugs, discloses an application of artemisinin, dihydroartemisinin and artesunate in the preparation of the drugs which are taken as the vincristine anti-tumor synergists and discloses an application of artemisinin, dihydroartemisinin and artesunate in the preparation of the drugs for treating oral squamous cell carcinoma, the applications of the present invention are proven to have great clinical significance by the trials.
US20110223248 Methods and compositions for treating lactose intolerance The invention provides methods and compositions for treating symptoms associated with lactose intolerance and for overall improvement in gastrointestinal health. Described herein are methods and compositions for improving overall gastrointestinal health or for decreasing symptoms of lactose intolerance by administering to subject in need thereof a lactose composition optionally in combination with effective amount of a probiotic, prebiotic, or both.
WO2014012849A1 A new crystal form of cefoperazone sodium The present invention relates to a new crystal form of cefoperazone sodium and the method for making said crystal form. The new crystal form has the following characteristics: orthorhombic crystal, space group F222, unit cell dimensions a=52.15Å, b=51.87Å and c=4.95 Å.
CN102911147A Novel compound, preparation method and application thereof and medicament composition and preparation of novel compound The invention discloses a novel compound 5,6,7-trihydroxy-4'-oxethyl flavone, a medicament composition and a preparation thereof and an application of the novel compound in preparing medicaments. The invention also relates to a preparation method of the compound which is obtained by reacting 5,6,7,4'-tetrahydroxy flavone with halogenated ethane in the presence of a catalyst. The method disclosed by the invention has the characteristics that the raw materials are available, the reaction conditions are gentle, the operation is simple, the product yield and purity are high, the production cost is low and the like, and is convenient to be used for industrial production. The compound disclosed by the invention has targeted therapeutic action on hyperuricemia, gout, arthritis and gouty arthritis, has the characteristics of high efficiency, low toxicity and high safety, and has wide application prospect.
EP1854464A2 Combinations comprising epothilone derivatives The invention relates to a pharmaceutical combination which comprises (a) an alkylating agent and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl, and Z is O or a bond. Said combination can be useful for the treatment of a proliferative disease, especially a tumor disease.
CN101716151A Finasteride oral tablets with quick dissolution and preparation method thereof The invention relates to finasteride oral tablets with quick dissolution and a preparation method thereof. The preparation is prepared by taking finasteride as a raw material medicament and adding auxiliary materials such as a filling agent, a disintegrant, a surfactant, an adhesive, a lubricant and the like. The adopted formula and preparation process not only ensure that the content uniformity of the preparation is easy to meet the requirement, but also ensure that the finasteride in the tablets can be quickly disintegrated and dissolved out in water, thereby greatly improving the dissolution of the medicament and playing a role in treatment more effectively.
WO2011063553A1 Traditional chinese medicine for treating flu induced by flu virus including type a h1n1 virus A traditional Chinese medicine for treating flu induced by flu virus including type A H1N1 virus, its preparation method and its use are disclosed. The traditional Chinese medicine said above is prepared by the crude materials including fried Herba ephedrae, Gypsum Fibrosum, Flos Lonicerae, Fructus Forsythiae, Radix Scutellariae, Rhizoma Anemarrhenae, Bulbus Fritillariae Thunbergii, fried Semen Armeniacae Amarum, Fructus Arctii, Herba Artemisiae, Herba Menthae, and raw Radix Glycyrrhizae. The preparation method of the traditional Chinese medicine said above includes boiling the crude materials in water, or crushing the crude materials into powder, or other conventional methods. The use of the traditional Chinese medicine said above is to prepare the drugs for treating flu induced by flu virus including type A H1N1 virus.
US7271172 Pyrrolidine and azetidine compounds as CCR5 antagonists The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).
CN103655559A Application of incarvillateine compounds in preparation of anti-breast cancer drugs The invention relates to the technical field of medicine, in particular to application of incarvillateine compounds in preparation of anti-breast cancer drugs. Two kinds of methods, namely an operative treatment method and a drug treatment method, can be used for treating breast cancer at present, however, breasts are usually needed to be excised in the operative treatment method, which does serious harm to bodies and minds of women, while the side effect of the drug treatment method is large. Incarvillateine compounds can inhibit the activity of a breast cancer cell MCF-7 and RhoGTOs family target cells, so that after the incarvillateine compounds are applied to the preparation of anti-breast cancer drugs, the growth speed of tumors can be effectively reduced, the lifetime of a patient can be prolonged and the side effect is slight.
US20090130225 Macrolides derivatives as antibacterial agents The present invention provides macrolide derivatives, which can be used as antibacterial agents. Compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram-positive, gram-negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Propionibeacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds described herein, pharmaceutical compositions thereof, and methods of treating bacterial infections.
US20080085242 modified biodegradable branched chitosans effectively complexed with nucleic acids The present invention concerns a novel composition comprising a nucleic acid; and a chitosan containing branching groups covalently linked to the amino groups wherein said branches are selected from the following groups; alkyl with 2 or more carbon atoms, monosaccharides, oligosaccharides or polysaccharides. The composition is particularly useful as a non-viral gene delivery system. The composition facilitates the introduction of the nucleic acid into the cells to which it is administrated, as well as the expression of the function of the nucleic acid.
CN1850083A Dispersible tablet for treating cold and its preparing process The present invention relates to a dispersion tablet for curing common cold and its preparation process. Said invention is formed from main medicine including paracetamol, pseudoephedrine hydrochloride, dextromethorphan and chlorpheniramine maleate and auxiliary medicine including avicel, low-substituted hydroxypropyl cellulose, povidone K30, cross-linked povidone, aspartame, aspartame, micropowder silica gel and magnesium stearate.
CN101066963A Polysubstituted flavanone derivative and its prepn and application The present invention provides one kind of nitrogen atom-containing polysubstituted flavone derivatives, 2-substituent phenyl-5, 7-dioxy-8-amino methylene flavone derivatives, which are synthesized through introducing different amino methylene structures into the 8-position of flavone kernel. Pharmacological activity experiments shows that the 2-substituent phenyl-5, 7-dioxy-8-amino methylene flavone derivatives have certain antitumor activity, high selectivity and cell period inhibiting effect and may be applied in antitumor medicine. The present invention has the general structural expression of the 2-substituent phenyl-5, 7-dioxy-8-amino methylene flavone derivatives shown.
US20090209632 Percutaneously Absorptive Ophthalmic Preparation Comprising Olopatadine The present invention provides a percutaneously absorptive preparation for preventing or treating allergic eye disease, which comprises olopatadine or a salt thereof as an active ingredient. In addition, the present invention provides a method for preventing or treating allergic eye disease, which comprises applying a percutaneously absorptive preparation comprising olopatadine or a salt thereof to the skin surface including the skin surface of an eyelid, thereby casing transfer of a therapeutically effective amount of olopatadine or a salt thereof from the preparation to an anterior ocular segment through the skin of the eyelid rather than a systemic blood flow. The present preparation can exert a pharmacological effect over a prolonged period by a single application, as compared to conventional preparations such as eye drops.
EP1439176B1 Pyrimidone compounds and pharmaceutical compositions containing the same The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A1, A2A, and A2B receptors), particularly, compounds represented by the general formula (I), salts thereof, or solvates of both: (I) wherein R1 and R2 are each independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a C6-14 aromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, C1-6 acyl, or C1-6 alkylsulfonyl; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl; R4 is a C6-14 aromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and R5 is a C6-14 aromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).
WO2009013299A3 Novel bradykinin b1 antagonists The present invention relates to compounds of the general formula (I), in which A, Y, R1, R2, R3, R4 and R5 are as defined in claim 1, the enantiomers thereof, the diastereomers thereof, mixtures thereof and salts thereof, especially physiologically tolerated salts thereof with organic or inorganic acids or bases, which have valuable properties, to the preparation thereof, to medicaments comprising the pharmacologically active compounds, the production thereof and the use thereof.
WO2011162234A1 Composition which is used for purpose of inhibiting biosynthesis of cholesterol It has been found that dolichoic acid or a precursor thereof has cholesterol biosynthesis inhibitory activity and is extremely useful as a composition such as a pharmaceutical product, food or drink for lowering the blood cholesterol level.
CN102531868A Anthraquinone derivative, preparation method and application thereof The invention relates to an anthraquinone derivative, a preparation method and application thereof. During preparation, entomopathogenic fungi in soft coral Alternaria sp. (ZJ-2008003) is first placed in a strain culturing medium for strain culturing and then placed in a fermentation culturing medium for fermentation culturing, obtained fermentation liquor is filtered, thalli are removed to obtain filtrate, and the filtrate is extracted through ethyl acetate; after extract liquor is concentrated, silicagel column chromatography, sephadex LH-20 gel column chromatography and half-preparation of high performance liquid chromatography preparation are conducted, obtained eluent is concentrated, and clear crystals are obtained, namely, the compound of tetrahydroaltersolanols C-E; pink powder is obtained, namely, the compound of tetrahydroaltersolanol F. The anthraquinone derivative originating from marine fungi has strong antiviral effect, can effectively restrain porcine reproductive and respiratory syndrome virus (PRRSV), can be used as antiviral drug, and has broad application prospects due to the fact that raw materials can be produced in a large scale.
EP1071403B1 Pharmaceutical composition containing a statin and aspirin A pharmaceutical composition is provided which is useful for cholesterol lowering and reducing the risk of a myocardial infarction, which includes a statin, such as pravastatin, lovastatin, simvastatin, atorvastatin, cerivastatin or fluvastatin, in combination with aspirin, in a manner to minimize interaction of aspirin with the statin and minimize side effects of aspirin. A method for lowering cholesterol and reducing risk of a myocardial infarction employing such composition is also provided.
EP1622874B1 3,4-dihydro-1h-quinolin-2-one derivatives as norepinephrine reuptake inhibitors This invention relates to compounds of formula (I) where -X-, n, R1, R3 and Ar- have the values defined herein, their preparation and use as norepinephrine reuptake inhibitors useful for the treatment of nervous system disorders
CN101391049A Medicine for curing epilepsy The invention discloses a medicine for curing epileptic, which is composed of the following materials by weight ratio: gen-seng, Atractylodes macrocephaia, Tuckahoe, cinnamon, aconite, Dried Human Placenta, walnut meat, mulberry, arillus longan, Deerhorn Gelatin, radix paeoniae alba, amber, rhizoma gastrodiae, polygala, uncaria, benzoin, magnetite, strychnos alkaloids, muskiness, hawkthorn and costus root. The medicine has obvious effect for curing the epileptic, can rapidly improve the epileptic symptom, has accurate curative effect after using the medicine, has no side effects and has effect after using the medicine 1 treatment period later; the light patients can be treated in 3 treatment periods (60 days for each treatment period); and the heavy patients can be treated in 6 to 9 treatment periods; and the medicine can be used for long time after recovery.
CN1915216A New usage of tandospirone and its derivative, and composition containing tandospirone An application of the tandospirone and its derivatives in preparing the locally applied medicine for treating anxiety by sublingual mucosa absorption is disclosed.
US7759367 Pharmaceutical compositions and their uses The present invention relates to compositions comprising 1,2-dihydropiridin-2-one compounds and an immunoregulatory or anti-inflammatory agent. The compositions are useful for the prevention or the treatment of neurodegenerative diseases, for example demyelinating disorders.
CN102875628A (20S,24S)-ocotillol ginsenoside derivatives with antibacterial activity, and preparation method and application thereof The invention relates to the fields of organic synthesis and pharmacochemistry, particularly (20S,24S)-ocotillol ginsenoside derivatives, of which the structure is disclosed as general formula (I). The invention also discloses a preparation method of the (20S,24S)-ocotillol ginsenoside derivatives, a pharmaceutical composition containing the (20S,24S)-ocotillol ginsenoside derivatives, and application of the (20S,24S)-ocotillol ginsenoside derivatives in bacterial infection disease inhibition. General formula (I).
US20100310595 Method of transfection and compositions therefor The present invention relates to the targeted delivery of molecules to cells expressing toll-like receptors (TLRs). Aspects of the invention provide compounds comprising a positively charged group linked to a TLR ligand. These compounds are useful for in vitro and in vivo methods of transfection of TLR-expressing cells. Other aspects of the invention relate to the use of such compounds for repression of gene expression and DNA vaccination approaches.
CN101810585A Invertose (fructose/glucose) medicinal composition microsphere injection The invention discloses an invertose (fructose/glucose) medicinal composition microsphere injection, which is characterized by comprising the following components in part by weight: 1 part of glucose, 1 part of fructose, 3 to 8 parts of albumin and 0.8 to 2 parts of PEG 600. Compared with the prior art, the prepared invertose (fructose/glucose) medicinal composition microsphere injection has the advantages that: the stability is good, the encapsulation rate is high and a preparation process is suitable for industrial production; and the glucose has the appropriate controlled-release effect that the release amount does not exceed 30 percent within 1 hour, the release amount is between 50 and 70 percent within 6 hours, the release amount is between 65 and 85 percent within 12 hours and the release amount is not less than 80 percent within 18 hours.
CN102940637A Isoniazid-rifampicin-anethol trithione composition and its oral preparation The invention provides an isoniazid-rifampicin-anethol trithione composition and its oral preparation, relating the technical field of medicines and medicine making. The composition contains 0.1-99.9wt% of isoniazid, 0.1-99.9wt% of rifampicin and 99.9-0.1wt% of anethol trithione. According to the invention, isoniazid, rifampicin and anethol trithione have good synergistic effect, the capacity of anethol trithione in raising cellular capabilities increases biliation, thus liver damage caused by isoniazid and rifampicin can be effectively treated; the combined use of isoniazid, rifampicin and anethol trithione can reduce the adverse reaction caused by isoniazid and rifampicin, reduce liver damage, and has good therapeutic effect on tuberculosis patients.
WO2010066253A8 Selective inhibitors of excitatory amino acid transporter subtype 1 (eaat1 /glast) The invention is the discovery of the use of the class of compounds represented by Formula I, as selective inhibitors of excitatory amino acid transporter (EAAT) subtype (EAATl) and its rodent ortholog L-glutamate/L-aspartate transporter (GLAST).
CN101631549B Process for production of buprenorphine pharmaceutical preparation to be applied to mouth mucosa The invention aims at providing a process for the production of a buprenorphine pharmaceutical preparation to be applied to mouth mucosa. The process is characterized by comprising the step of preparing granules for rapid release layer containing buprenorphine hydrochloride crystals whose 90% cumulative diameter is 200[mu]m or below, the step of preparing granules for sustained release layer containing buprenorphine hydrochloride crystals whose 90% cumulative diameter is 250[mu]m or below, and the step of compressing both the granules into double-layer tablets.
CN1586494A Helicidum oral disintegation tablet and its preparing method The present invention discloses orally disintegrated helicidum tablet suitable for remitting neurosis with headache, dizziness and sleep trouble and auxiliarily treating primary headache. The orally disintegrated tablet is prepared with helicidum as main material, and through adding stuffing, disintegrating agent, corrective, flow assistant and other supplementary material, and other special steps. The present invention has the features of simple preparation process, fast disintegration, fast acting, etc.
WO2005066173A3 Processes for the preparation of substituted azetidinone A novel intermediate compound of formula (II) wherein R1 is an oxygen protecting group can be use in an efficient process for making certain carbapenem compounds useful as anti-bacterial agents.
WO2013001786A1 Eye fatigue suppression composition and food and drink containing same The present invention provides an eye fatigue suppression composition having resveratrol as an active ingredient. As a result of extensive research, the inventors of the present invention discovered that resveratrol has an eye fatigue suppression effect and brought to fruition this eye fatigue suppression composition having resveratrol as an active ingredient. This composition is absorbed through the oral cavity and acts immediately to suppress eye fatigue.
WO2008004542A1 Method of separating vesicle, process for producing medicinal preparation, and method of evaluation A method of separating vesicles whose membrane has been modified with a hydrophilic polymer (polyethylene glycol, etc.). In the method, vesicles (liposome, etc.) differing in the degree of membrane modification are separated by ion-exchange chromatography using a concentration gradient in which the ionic intensity of an eluent is changed with time. Also provided are: a process for producing vesicles purified so as to have a desired degree of modification with a hydrophilic polymer which comprises utilizing the separation method in the step of purifying vesicles; a method of evaluating a medicinal vesicle preparation containing a drug therein, the method comprising using the separation method; and vesicles in which the membrane has been modified with a hydrophilic polymer and which include no vesicle having a degree of membrane modification less than 0.5 mol%.
CN103251950A Use of S1P receptor conditioning agent on preventing and curing intestinal radiation sickness and radiation enteritis The invention relates to a method of using an S1P receptor conditioning agent to prevent and/or cure stomach and intestine organization damages caused by ionising radiation, concretely to individually use, or combined with other treatment methods, the S1P receptor conditioning agent to prevent and/or cure intestinal radiation sickness and radiation enteritis caused by tumour radiation treatment.
CN101439151B Medicament for treating beriberi The invention relates to a drug for treating beri-beri which is characterized in that the drug is prepared by the following raw materials by parts by weight: 5-7 parts of pangolin scales, 5-7 parts of tremella fuciformis dried product, 6-8 parts of bletilla striata, 7-8 parts of golden thread, 15-20 parts of borneol, 10-12 parts of Szechuan lovage rhizome, 3-5 parts of plant ash, 2-5 parts of cicada slough, 4-6 parts of holly leaf fresh product, 2-4 parts of natural indigo, 3-5 parts of siberian cocklebur herb dried product, 8-10 parts of manchurian wildginger, 6-9 parts of densefruit pittanyroot-bark, 10-12 parts of lightyellow sophora root, 8-10 parts of fennel fruit, 5-7 parts of yanhusuo, 3-5 parts of myrrh, 6-8 parts of Chinese angelica, 5-7 parts of trogopterus dung, 10-12 parts ofwhite vinegar, 5-10 parts of garlic and 15-20 parts of common salt. The drug has the advantages that the drug can rapidly relieve the itch and the pain, rapidly heal the wound and be effective by 1-2times, patients with the moderate beri-beri can be healed in 6 days, the patients with the severe beri-beri can be healed in 30 days, and the drug has no side effects, good efficacy, rapid onset of action, ability of radically curing the beri-beri, difficult recurrence, no complications or sequelae and low cost.
US20110286995 Drug Therapy for Celiac Sprue Administering an effective dose of a tTGase inhibitor to a Celiac or dermatitis herpetiformis patient reduces the toxic effects of toxic gluten oligopeptides, thereby attenuating or eliminating the damaging effects of gluten.
CN101348527A Production and powdering process of sodium carboxymethylstarch, and use thereof The invention provides a technology for producing a pulpy and powder-like raw material for carboxylmethyl with a pulpy intermediate of starch sodium carboxylmethyl. However, the technology must be provided with: (1) a specific room, (2) a specific pulp technology and, (3) a specific pulverization technology. Treatment procedures of chemical reactions and delicate technology are adopted. The obtained pulpy and powder-like starch sodium carboxylmethyl are used as raw materials. The technical indexes of the raw materials are that the content of sodium carboxylmethyl should be more than 6.5 percent, the specific rotation should be more than +160 degree, the specific viscosity is between 10 and 60, and the yielding rate should be more than 92 percent. Various formulations can be subsequently prepared for treatment of diseases and regulation on immune of both animals and human being, in order to prolong human life span.
EP2760852A1 Improved process for the preparation of sulfamide derivatives The present invention is directed to an improved process for the preparation of sulfamide derivatives.
US7002022 treatment of neoplastic diseases that respond to inhibition of the vascular endothelial growth factor receptor tyrosine kinase activity; tumors, retinopathy, macular degeneration Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R2 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
CN102936291A Method for preparing selenylation poly mannuronic acid and application of selenylation poly mannuronic acid The invention relates to the technical field of selenylation polysaccharide and provides a method for preparing selenylation poly mannuronic acid. The method comprises steps of suspending poly mannuronic acid in an anhydrous organic solvent; adding a sulfur trioxide-pyridine compound dissolved by the anhydrous organic solvent with stirring; conducting reaction for 1-10 hours at the constant temperature from 20 DEG C to 100 DEG C; adding ethanol; centrifugalizing a reaction product; cleaning by using the ethanol; adding water and dissolving; adjusting the Potential of Hydrogen (PH) value to the neuter by using alkali; conducting dialysis; conducting filtering; conducting freezing and drying; obtaining sulfonated poly mannuronic acid; subjecting the sulfonated poly mannuronic acid and selenite to the reaction in the acid solution at the catalysis of Ba2+; adding sulphate; extracting supernatant fluid through centrifugation; adjusting the Potential of Hydrogen (PH) value to the neuter by using the alkali; conducting dialysis; conducting filtering; conducting freezing and drying; and obtaining the selenylation poly mannuronic acid. The invention also provides application of the selenylation poly mannuronic acid which is prepared through the method in medicines and health products for prevention and curing of Alzheimer's disease.
CN102770416A Metaxalone cocrystals The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalore adipic acid cocrystal, a 1:0.5 metaxalore fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them.
CN103611214A Needle drug microsystem and preparation method thereof The invention belongs to the technical field of microneedle transdermal drug delivery, and relates to a needle drug integrated microsystem and a preparation method thereof. The method comprises the steps of dissolving drugs like baicalin or insulin in a coating solution, adding the coating solution containing the drugs into a microneedle by means of methods of dip coating or spray coating or spin coating and the like, and obtaining the needle drug integrated microsystem after drying. The needle drug integrated microsystem can be used for transdermal drug delivery, overcome the first-pass effect, caused by the traditional oral drug delivery, on the intestines and stomach, reduce stimulus to the intestines and stomach, have the better targeted advantage and the independent drug delivery advantage, overcome the barrier action, caused by cuticles, on drug diffusion by means of the microneedle, and have the wide application range.
EP1153017B1 Bicyclic compounds and their use as integrin receptor ligands The invention is directed to physiologically active compounds of general formula (I): wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring; R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; L1 is an -R3-R4- linkage where R3 is alkylene, alkenylene or alkynylene and R4 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, -C(=Z?2)-NR5-, -NR5-C(=Z2)-, -Z2¿-, -C(=O)-, -C(=NOR?5)-, -NR5-, -NR5-C(=Z2)-NR5¿-, -SO¿2?-NR?5-, -NR5-SO¿2-, -O-C(=O)-, -C(=O)-O-, -NR5-C(=O)-O- or -O-C(=O)-NR5-; L2 is optionally substituted alkylene or alkenylene; Y is carboxy or an acid bioisostere; and Z?1 is NR5¿; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).
CN103251578A Application of danshinolic acid A for preparing medicament for preventing and treating alzheimer disease The invention discloses compound danshinolic acid A with the activity of depolymerization and inhibition of production, aggregation or fibrillation of beta-amyloid proteins. Meanwhile, the compound can also be chelated with metal ions. As a beta-amyloid protein aggregation and inhibition active agent, the compound shows no toxicity on nerve cells and is capable of reducing Abeta-induced cytotoxicity; and as a metal ion chelating agent, the compound can be used for inhibiting Abeta aggregation induced by the metal ions. The compound disclosed by the invention is rich in sources and easy to be separated from red-rooted salvia roots and can be used for preparing a medicament for preventing or treating alzheimer disease.
CN101108200A Composition of starwort sulphonic acid or vitriolic acid polyoses ester total phenolic glycoside and method of preparing the same and antiviral application The invention relates to a kind of natural medicine of broad spectrum antibiotic. At present, the broad spectrum antibiotic medicine with high effect and safety is at shortage all round the world. The invention is intended to extract laminarinsulphate or sulphonic acid sugar ester or sulphosalts from plant chickweed or other chickweed plant with two resin adsorption methods or a water extraction and alcohol precipition method. The spectrum antibiotic in the invention is distributed under 50,000 in the formula weight formed by carbon glycosidic bond and/or oxide glycosidic bond with phenol, especially the total flavones comprising apigenin. However, the invention mainly acts as total phenolic glycoside with the formula weight under 4,000. Besides, the invention can form brownish compound with the total flavones comprising apigenin and the glycosidic ingredients without sulfur element, so as to be applied as broad spectrum antibiotic drug. Therefore, the compound in the invention can be applied to cure ADIS virus, hepatitis virus, influenza virus and parainfluenza virus comprising SARS, adenovirus, verruca acuminate virus, enterovirus, mumps virus, herpes simplex virus, herpes zoster virus and varicella. No toxic effect has been found in the application. What is more, the invention can be made into 10 sorts of formulation, disinfector and health-improving products.
CN103508957A Hydroxyethyl pyrazole compound or aminoethyl pyrazole compound, preparation method and use thereof The present invention discloses a hydroxyethyl pyrazole compound or aminoethyl pyrazole compound represented by a general formula I, a preparation method and a use thereof. Bioactivity test results demonstrate that the compound has significant beta-secretase inhibition activity, such that the hydroxyethyl pyrazole compound or aminoethyl pyrazole compound can be used as a beta-secretase inhibitor so as to be used for prevention or symptomatic treatment of senile dementia.
US20080260774 Activation cytokine response in immune system including lymphocyte and antigen; anticancer agents; infection diseases; autoimmune disease; vaccine The present disclosure relates to synthetic alpha-galactosyl ceramide (α-GalCer) analogs, and their use as immunotherapies. In one aspect, a method of activating a cytokine response in a subject includes administering an effective amount of a compound to a subject, wherein the subject has an adaptive immune system that includes a population of cells, the population including at least one lymphocyte and at least one antigen-presenting cell, and wherein the compound is represented by the structure of formula 1: wherein, n is 0 to 25; X is selected from O and S; R1 is selected from H, CH3, and phenyl, where phenyl is optionally substituted with H, OH, OCH3, F, CF3, phenyl, phenyl-F, C1-C6 alkyl, or C2-C6 branched alkyl; R2 is selected from OH and H; R3 is selected from C1-C15 alkyl, and phenyl, where phenyl is optionally substituted with H, OH, OCH3, F, CF3, phenyl, C1-C6 alkyl, or C2-C6 branched alkyl; R4 is selected from OH, OSO3H, OSO3Na, and OSO3K; and R5 is selected from CH2OH and CO2H; or a pharmaceutically acceptable salt thereof; forming a complex between the compound and the antigen-presenting cell, wherein the formation of the complex results in the activation of a receptor on the lymphocyte; and activating the lymphocyte to produce the cytokine response.
US20080025916 Tailored Treatment Suitable for Different Forms of Mastocytosis The present invention relates to a method for a tailored treatment of mastocytosis comprising a) assessing whether or not a c-kit mutation at position 816 is detected in a sample of a patient and b) administering a specific 816 mutant c-kit inhibitor in case a mutation is detected in step a) or an inhibitor displaying efficacy on c-kit wild in case no mutation is detected in step a). The invention is more particularly suited 10 for treating category II, III and IV mastocytosis.
WO2013060653A1 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes This invention relates to novel 1-cycloalkyl- or l-heterocyclyl-hydroxyimino-3-phen propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
CN101077347A Multifunctional membrane used for glaucoma post-operation and preparation method thereof The present invention relates to medicine technology, and is especially one kind of eye implant with slowly released active component and post-operational adhesion preventing function. The eye implant consists of chitosan derivative and medicinal active component mainly, and is prepared into film implanted into eye tissue to slowly released active component and to avoid adhesion before degradation, needing no taking out. It is used mainly after glaucoma treating operation and has high medicine bioavailability.
WO2010129053A8 Egfr inhibitors and methods of treating disorders The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
WO2013151490A1 Methods and compounds for treating diseases The present invention provides a method for amplifying an immune response in an individual, comprising altering the composition of FoxP3 isoforms by inducing an expression of a FoxP3 isoform, such as FoxP3d2d7, that inhibits the function of FoxP3fl and/or FoxP3d2, and a method for treating a cancer or an infection or for inducing an increased vaccine response in an individual, comprising amplifying an immune response in said individual, compounds for use in such methods, pharmaceutical compositions, and a method for in vitro testing of a candidate medicinal product. The invention further relates to a method for diagnosing inflammatory bowel disease (IBD) in an individual, and use of FoxP3d2d7 as a diagnostic marker for IBD.
WO2014118039A1 Radiolabeled compounds The present invention relates to radiolabeled compounds of formula (I) wherein R1, R2, R3 and R4 are as defined herein.
CN102883733A AGE production inhibitor Disclosed is an AGE production inhibitor or the like, which effectively inhibits the production of an advanced glycation end product (AGE), while having improved biological safety. Specifically disclosed is an AGE production inhibitor or the like, which contains an extract of cherry (preferably blossoms or leaves thereof) and/or a processed product of the extract as an active ingredient. The AGE production inhibitor or the like contains, as an active ingredient, at least one compound that is selected from the group consisting of 1-O-(E)-caffeoyl-ss-D-glucopyranoside, 1-O-(E)-coumaroyl-ss-D-glucopyranoside, 1-O-(E)-cinnamoyl-ss-D-glucopyranoside, kaempferol 3-O-ss-D-glucopyranoside, quercetin 3-O-ss-D-glucopyranoside, kaempferol 3-O-(6"-malonyl)-ss-D-glucopyranoside, and quercetin 3-O-(6"-malonyl)-ss-D-glucopyranoside.
CN103006677A Application of tree-sourced hetero-bignonia neo-glycoside II on preventing and treating neurodegenerative diseases Disclosed is the application of natural tree active ingredient hetero-bignonia neo-glycoside II on preventing and treating neurodegenerative diseases. The hetero-bignonia neo-glycoside II is one of main active ingredients of paulownia trees and has a molecular formula of C29H36O16. Experiments show that the hetero-bignonia neo-glycoside II has a protective effect on oxidative stress injuries of hydrogen peroxide induced rat adrenal pheochromocytoma cell PC12. Consequently, the hetero-bignonia neo-glycoside II can be used as medicines for preventing and treating the neurodegenerative diseases and can be prepared into various formulations with medicinal carriers.
CN103212094A Oxygen-fluorine liposome microbubble and preparation method thereof The invention discloses an oxygen-fluorine liposome microbubble therapeutic agent which consists of microbubbles, and oxygen and at least one perfluocarbon existing in the microbubbles, wherein the gas nucleus takes oxygen as a principle component and takes perfluocarbon as an auxiliary component, and the microbubble mainly consists of phospholipid and polyethylene glycol derivative. According to the oxygen-fluorine liposome microbubble therapeutic agent, oxygen can be controlled to be released in a human body through veins delivery and targeted hypoxia tissue under ultrasound wave irradiation, the hypoxia disease is treated, and the therapeutic agent serves as a contrast agent used for ultrasonic enhanced imaging. Therefore, the microbubble is a developing agent and an oxygenating therapeutic agent.
US20090042914 Delayed release formulations of 6-mercaptopurine The present invention provides enterically coated formulations of 6-mercaptopurine that exhibit a delay in release of the 6-mercaptopurine such that substantial release of 6-mercaptopurine does not occur until after passage through the stomach. Optionally, the formulations also comprise a delay coating in addition to the enteric coating that provides an even further delay such that substantial release of 6-mercaptopurine does not occur until after a certain period of time following passage through the stomach. Such a period of time is preferably at least one hour after passage through the stomach. Following the delay imparted by the enteric coating and optional delay coating, the formulations exhibit better bioavailability and faster dissolution than previous formulations.
US20110144124 Compounds and Compositions for Use as Modulators of Tau Aggregation and Alleviation of Tauopathies This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.
WO2013118949A1 Phenyl derivatives or pharmaceutically acceptable salts thereof, method for preparing same, and composition comprising same as active ingredients for preventing, improving or treating diseases related to vascular endothelial cells or diabetes The present invention relates to phenyl derivatives or to the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a composition comprising same as active ingredients for preventing, improving or treating diseases related to vascular endothelial cells such as diabetes and diabetic complications. The phenyl derivatives according to the present invention may effectively regulate glucose use, have excellent effects in inhibiting the production of advanced glycation end-product which is a causing factor in diabetic complications, have superior effects in treating (preventing) the pathological widening of the diameter of a vitreous body vessel by hyperglycemia in an animal model (zebra fish), prevent a destruction of a blood-retinal barrier in a diabetic retinopathy-induced animal model (SD rat), increase occludin, which is a protein constituting a tight junction, and significantly reduce pathologically-increased vascular endothelial growth factors. Therefore, the phenyl derivatives of the present invention may be effectively used as a composition for preventing, improving or treating diseases related to vascular endothelial cells, such as diabetes and diabetic complications.
US20110288172 Dermatological compositions and methods Dermatological compositions (methods of making and using) that include one or more anesthetic agents and/or one or more anti-inflammatory agents and/or a combination of ammonium, sodium, and potassium salts, preferably of an alpha-hydroxy acid.
WO2009115652A3 Bitherapy and tritherapy used for treating an hiv-positive patient The invention relates to a composition that comprises an anti-HIV treatment and a treatment for the side effects of said anti-HIV treatment for a patient affected by HIV. The invention can particularly be used in the treatment of the side effects generated by certain anti-HIV treatments, such as early aging, lipodystrophy, which can be generated by protease inhibitors or reverse transcriptase inhibitors. The composition of the invention includes at least one inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, at least one inhibitor of farnesyl-pyrophosphate synthase, and at least one anti-HIV agent. One of the methods for treating a patient infected by HIV comprises the following steps in any order: (i) administration of a mixture containing at least one inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase and at least one inhibitor of farnesyl-pyrophosphate synthase; and (ii) administration of an anti-HIV agent, wherein the administrations are concomitant, consecutive, or alternating.
CN1957921A Controlled release injection of carried fluorouracil and synergis A slowly-release anticancer medicine in the form of injection or implant is disclosed. Said slowly-release injection is composed of a special solvent containing suspending aid and the slowly-release microballs consisting anticance medicine, iterstitial hydrolyte and slowly-releasing auxiliary. Said anticancer medicine is chosen from 5-FU, genoxal, etc. Said interstitial hydrolyte is chosen from collagenase, relaxin, etc. Said slowly-releasing auxiliary is chosen from polylactic acid, FAD, polyethanediol, etc.
US20090156593 Spirocyclic Azaindole Derivatives The invention relates to substituted azaindole derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted azaindole derivatives for producing medicaments.
US7648992 Metalloproteinase 9 and/or 12 inhibitors; such as 5-({[4-[(2-cyclopropylpyrimidin-5-yl)ethynyl]-3,6-dihydropyridin-1(2H1)-yl]sulfonyl}methyl)-5-methylimidazolidine-2,4-dione; synthesis; asthma, chronic obstructive pulmonary disease The invention provides compounds of formula (I), wherein R1 and R2 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
EP1486208B1 Use of a novel preventive for infections It is intended to provide a preventive efficacious against infections, an agent potentiating the effect of preventing infections of cystine; and foods and feeds efficacious against infections. Namely, a preventive efficacious against infections which comprises a combination of cystine or the like with teanine; an agent potentiating the effect of preventing infections of cystine or the like which contains teanine; and foods and feeds efficacious against infections which comprise a combination of cystine or the like with teanine.
US20100272752 Vaccine for viruses that cause persistent or latent infections The invention is in general directed to methods and compositions for preventing or treating infections by viruses involved in persistent and/or latent infections. The methods and compositions are directed toward the prevention and treatment of infections caused by viruses such as, for example, herpesviruses, retroviruses, hepatitis viruses, and papillomaviruses, including, for example, cytomegalovirus.
EP1808172A2 Botanical extract compositions and methods of use A composition having phytoestrogenic and anti-cancer activity is described. The composition comprises wogonin, isoliquiritigenin, coumestrol, their pharmaceutically acceptable salts or esters, their selectively substituted analogs, or combinations thereof. The compositions may also include an anti-cancer agent and/or an immune stimulant. A method for treating or preventing cancer or an estrogen related disorder includes administering a therapeutically effective amount of the compositions is described. The compositions are particularly useful in the treatment of hormone-related cancers
WO2005039546A2 Use of indoleacetic acid derivatives which increase the serum igf-1 level for the preparation of a therapeutical composition for treatment of various diseases The present invention relates to the use of one or more compounds that are capable of increasing the serum level of insulin-like growth factor 1 (IGF-1) for the preparation of a therapeutical composition, in particular in the form of a food supplement, for the treatment of subjects suffering from serious fatigue and exhausting symptoms, burn-out and chronic fatigue syndrome. The same composition can also be used by patients suffering from depression, Alzheimer disease, irritated bowel syndrome, osteoporosis, type 2 diabetes, or for anti-aging, immune therapy and recovery after exercise. The composition also has a use in veterinary applications for increasing the growth and immunity in animals.
CN101829141A Application of scallop polysaccharide in preparation of anti-herpes simplex virus medicament The invention relates to application of scallop polysaccharide in the preparation of an anti-herpes simplex virus medicament, which comprises the following steps of: preparing 5 mass percent solution of scallop polysaccharide by using distilled water, absorbing the solution of scallop polysaccharide through an active carbon, and heating the solution; centrifuging and filtering the solution; performing ultrafiltration on the filtrate by using 100k and 5k filter membranes sequentially; performing the freeze drying of the filtrate to obtain the light yellow powder-type purified scallop polysaccharide with a molecular weight of between 5 and 100k; and grinding the purified scallop polysaccharide and screening the ground scallop polysaccharide with an 80 mesh screen, and uniformly mixing the ground scallop polysaccharide with a medical starch in the weight ratio of 1:1-10 to prepare 50mg or 100mg of capsules; or grinding the purified scallop polysaccharide and screening the ground scallop polysaccharide with an 80 mesh screen to prepare 50mg or 100mg of tablets by a wet palletizing process. The scallop polysaccharide is the natural product, and has the advantages of low toxicity, light side effect, high safety and excellent anti-herpes simplex virus effect.
US20120283310 MicroRNA Signatures Associated with Human Chronic Lymphocytic Leukemia (CLL) and Uses Thereof Methods and compositions for the diagnosis, prognosis and/or treatment of leukemia associated diseases are disclosed.
CN101612324B Medicament for treating cerebral thrombosis The invention discloses a medicament for treating cerebral thrombosis, which comprises the components of Radix Notoginseng, Salvia miltiorrhiza, achyranthes, prepared rehmannia root, radix paeoniae alba, medlar, rhizoma gastrodiae, polygala, root of straight ladybell, dogwood, fossilia ossis mastoid, oyster, tortoise plastron, saffron, sealwort, raw hawthorn, Endothelium Corneum Gigeriae Galli and dried orange peel. The medicament for treating cerebral thrombosis has the advantages of obvious effect on treating cerebral thrombosis, good curative effect, high cure rate and no toxic or side effect after long-term administration, and is an ideal medicament for treating cerebral thrombosis. The medicament for treating cerebral thrombosis has the effective rate of 89%, and the cure rate of 75%.
EP2657233A1 3,5-disubstituted alkynylbenzene compound and salt thereof The present invention provides a compound represented by Formula (I) (wherein R1, X1, X2, Y, and Z are as defined in the specification), or a salt thereof.
CA2145535C Adenovirus vectors for the transfer of foreign genes into cells of the central nervous system, particularly in brain The invention concerns a recombinant DNA vector characterized in that it is capable of directing the expression and/or transcription of a selected nucleotide sequence in the cells of the central nervous system and in that it comprises (i) at least part of the genome of an adenovirus, including the regions required for that adenovirus to penetrate into the cells normally infectable by that adenovirus and (ii) being inserted into said part of genome of an adenovirus under the control of a promoter, either present or also inserted into said genome part and operative in said cells. This recombinant vector finds particular use in the treatment of diseases of the central nervous system, also in gene therapy.
EP0978284B1 Use of 15-keto-prostaglandin-e compounds as endothelin antagonists An antagonist against endothelin believed to relate to the causes of diseases such as hypertension, Buerger's disease, asthma, eyeground diseases, and the like. The antagonist comprises a 15-ketoprostaglandin E compound, especially, a 13,14-dihydro15-keto-16-mono- or dihalogenoprostaglandin.
WO2013111924A1 Novel compound derived from ishige foliacea, and use thereof The present invention relates to octaphlorethol A, a novel compound which is isolated and identified from Ishige foliacea, to a method for preparing same, and to the use of octaphlorethol A for preventing or treating metabolic diseases including diabetes. The octaphlorethol A compound of the present invention can prevent and treat diabetes and complications of diabetes caused by hyperglycemia since the octaphlorethol A compound reduces blood glucose in an animal model, has excellent activity in inhibiting carbohydrate digestive enzymes, and has the effect of facilitating the uptake of glucose in the muscles. Also, the compound of the present invention can be used in the prevention and treatment of various types of metabolic diseases caused by other metabolic disorders since the compound has the activities of suppressing angiotensin converting enzyme (ACE) activation, adipocyte differentiation, and fat accumulation in cells.
CN1288147C Stable polymorph of FLIBANSERIN, technical process for its preparation and the use thereof for preparing medicaments This invention relates to the polymorph A of flibanserin (1), to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.
US20110178048 Stabilized formulation of triamcinolone acetonide A stabilized formulation of triamcinolone acetonide in a bioadhesive base material is provided. The present invention further includes a method of producing a stabilized non-aqueous TAA formulation and methods of measuring the stability of such TAA formulations.
US20100210581 Nucleoside Derivatives as Inhibitors of Viral Polymerases A class of nucleoside derivatives of formula (I), as defined herein, that are useful as inhibitors of RNA-dependent RNA viral replication and in particular HCV replication, are provided. Also provided are processes for the synthesis and use of such compounds for treating or preventing HCV infection.
US20100169994 Animal model The invention relates to the use of a NK1−/− animal as a model for attention deficit hyperactivity disorder and related conditions, to markers for those conditions and to methods of treating such conditions.
US20070249729 Method of Treating Elevated Plasma Homocysteine Levels in Esrd Patients A method of treating elevated plasma total homocysteine levels (tHc) in subjects with end stage renal disease (ESRD) is disclosed, said treatment comprising the administration of sodium 2-mercaptoethylsulfonate (MESNA) immediately prior to, or concurrently with, performing hemodialysis on said patient.
US20090148450 ATF4 As A Therapeutic Target In Alzheimers Disease And Other Neurological Disorders The present invention relates to methods and compositions for treating Alzheimer's Disease and other neurological disorders by inhibiting expression and/or activity of ATF4. It further provides for diagnostic methods and reagents as well as assays to identify agents for the treatment of Alzheimer's Disease and other ATF4-related conditions.
CN102451193A Eyewash for alleviating nyctalopia and preparation method thereof The invention relates to eyewash for alleviating nyctalopia and a preparation method thereof. The eyewash is characterized by being prepared from 20-40% of abalone shell, 10-30% of sodium chloride and 30-35% of natural vitamin A as main raw materials as well as 5-6% of pearl, 500 mL of distilled water and the like. The preparation method comprises the steps of: adding the raw materials except distilled water to a vessel according to the ratio, carrying out high-temperature treatment for 3-4 hours, sealing and soaking for 36 hours; and filtering out medicament liquid, adding distilled water according to a ratio of 1-7, and uniformly mixing. As compared with the traditional eyewash, the eyewash provided by the invention has no toxic or side effect and has no irritation to eyeballs, and can relieve eye fatigue, loosen eye muscle and alleviate nyctalopia.
WO2011097950A1 6-o-methylerythromycin 9-o-(3-hetroaryl-2-propenyl) oxime ketolide derivatives, preparation methods and pharmaceutical compositions thereof Compounds represented by general formula (I) or their pharmaceutically acceptable salts or esters with mineral or organic acids are disclosed. Wherein Ar is aromatic heterocyclic alkyl or substituted aromatic heterocyclic alkyl, and X is H or F. The preparation methods for compounds represented by general formula (I) and uses of theses compounds as anti-infective agents are also disclosed.
WO2012052556A1 Novel haloalkoxyquinazolines, and preparation and use thereof The invention relates to novel quinazoline derivatives which are suitable as diagnostic and therapeutic drugs and can be used especially for diagnosis and treatment of neurodegenerative and psychiatric disorders, for example schizophrenia. The novel quinazoline derivatives are notable for a high affinity and selectivity for PDE10A and by virtue of having at least one halogen-substituted substituent on the quinazoline radical.
EP1446162B1 Combination motif immune stimulatory oligonucleotides with improved activity A class of immunostimulatory nucleic acids having at least two functionally and structurally defined domains is provided. This class of combination motif immunostimulatory nucleic acids activates an immune response and is useful for treating a variety of immune realted disorders such as cancer, infectious disease, and allergic disorders. The nucleic acids also stimulate activation of natural killer cells and production of type 1 interferon.
CN102178632A Application of ozonized oil to preparation of raw materials of medical health-care products The invention discloses application of ozonized oil to preparation of raw materials of medical health-care products and belongs to the field of medical health care. In particular, the ozonized oil is applied to preparation of toothpaste for preventing and treating saprodontia and oral diseases, preparation of cosmetics for preventing all the skin infectious diseases, preparation of medical dressing for externally applying to surgical wounds and skin diseases and preparation of ointment applied to burnt wound surfaces and traumatic wound surfaces. The ozonized oil has unmatched effect on daily sterilization compared with any other bactericide and does not have toxicity and medicament tolerance.
US20110177084 Novel use application of sugar chain-recognizing receptor Provided are a novel means for regulating inflammatory reactions by regulating the signaling in inflammatory responses caused by non-homeostatic cell death, specifically an anti-inflammatory agent comprising a substance that inhibits the expression of Mincle or the interaction of Mincle and SAP130 or FcRγ, a screening method for a substance that regulates inflammatory reactions, comprising contacting Mincle or a fragment containing an extracellular region thereof and SAP130 in the presence and absence of a test substance, and comparing the degrees of the interaction of Mincle or the fragment thereof and SAP130 under the two conditions, a method of detecting non-homeostatic cell death, comprising measuring the amount of SAP130 in a sample collected from a subject animal, and the like.
US20050171061 Phenylsulfanylphenyl and phenyloxyphenyl substituted piperazine compounds; glycine transport inhibitors; for the treatment of psychoses and convulsive disorders: epilepsy, spasticity, and myoclonus The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.
US20110263672 Metabolites of Wortmannin Analogs and Methods of Using the Same Novel metabolites of wortmannin and wortmannin analogs and their use in inhibiting PI-3 kinase activity in mammals and the treatment and prevention of cancer or tumor formation in a subject are described herein.
CA2684853A1 Dietary supplement for promoting wellness and weight loss and methods of administering the same Disclosed herein are dietary supplements for promoting wellness and weight loss in a subject. In one aspect, the method includes administering to a subject whom wishes to lose weight a dietary supplement containing an extract product of Salacia, an extract product of Lagerstroemea speciosa, an extract product of French maritime pine bark, an extract product of Pterocarpus marsupium, and an extract product of Syzygium cumini, said composition being administered in an amount effective to promote wellness and weight loss in the subject.
US20080069889 Mixture of polysaccharide and binder; reverse agglomeration The present invention provides resilient self-adhering granules which comprise a polysaccharide present in an amount from about 10 wt % to about 90 wt % and a binder having a viscosity from about 5,000 mPa·s to about 250,000 mPa·s present in an amount from about 90 wt % to about 10 wt %, wherein the granule is capable of reversible agglomeration at or below 6,500 kilonewtons/m2. The present invention also provides oral dosage compositions comprising the resilient self-adhering granules and methods for making and using the resilient self-adhering granules.
US20100105667 Quinoxaline- and Quinoline-Carboxamide Derivatives The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
US20110053984 Novel 4-benzhydryloxy-tetraalkyl-piperidine derivatives and their use as monoamine neurotransmitter re-uptake inhibitors This invention relates to novel 4-benzhydryloxy-tetraalkyl-piperidine derivatives of Formula (I), any of its stereoisomers or any mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof, wherein Ra represents hydrogen or C1-6-alkyl; Rb and Rc independent of each other represent a phenyl group, which phenyl group is optionally substituted with one or more substituents independently selected from the group consisting of halo, trifluoromethyl, trifluoromethoxy, cyano, C1-6-alkoxy and methylenedioxo; R′, R″, R′″ and R″″ independent of each other represent C1-6-alkyl; and with the proviso that the compound is not 4-benzhydryloxy-1,2,2,6,6-pentamethyl-piperidine, useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
CN1839829A Antiviral cold compound formulation containing arbidol and taurine The invention relates to a compound preparation for resisting viral influenza containing arbidol and taurine, which can be prepared into any one of the pharmacologically acceptable dosage forms, especially solid oral administration medicaments.
US20110065739 Novel isoxazole drivative Disclosed is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which has an agonistic activity on GPR120 and is therefore useful for the treatment of diabetes, obesity or hyperlipemia. [In formula (I), the A represents a phenyl group which may be substituted by a lower alkoxy group or the like; the 13 represents a bivalent group produced by removing two hydrogen atoms from a benzene ring which may be substituted by a halogen atom or the like; X represents a lower alkylene group having 2 to 4 carbon atoms in its main chain or the like, wherein a carbon atom constituting the main chain may be substituted by an oxygen atom or the like; and Y represents a hydrogen atom or the like.]
WO2007044015A9 Treating or preventing renal cancer using a dimethane sulfonate The present invention features methods of treating renal cancer by administration of certain dimethylsulfonate compounds. The present invention further features administration protocols and dosing schedules for methods of treating patients suffering from renal cancer and pharmaceutical compositions suitable for use in the treatment methods provided herein.
EP1292568B1 Benzamide ligands for the thyroid receptor New thyroid receptor ligands are provided which have the general formula (I) in which: X is -0-, -S-, -CH2-, -CO-, or -NH-; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is methyl, ethyl, n-propyl or trifluoromethyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
US20100087537 Reduced irritant enema for the treatment of inflammatory bowel disease (ibd) The present invention comprises packaged enemas for the treatment of Inflammatory Bowel Disease (IBD), having substantially pure 5-ASA as the active ingredient, with a liquid carrier medium having a material avoidance of bowel irritant substances, such as anti-oxidants for the 5-ASA active ingredient, including such sulfites as potassium metabisulfite, for example, and contained within a sealed and substantially oxygen-free barrier package, which may preferably be formed of a foil/polymer laminate, and which package contains or otherwise includes an oxygen scavenger, such as a an oxygen scavenging sachet.
CN102309463A Ganciclovir tablet composition and its preparation method A ganciclovir tablet composition. The ganciclovir tablet composition comprises the following components of: by weight, 1part of ganciclovir hydrate crystals, 0.1-0.5 part of lactose, 0.05-0.08 part of hydroxypropylcellulose, 0.008-0.014 part of carboxyl methyl starch sodium, a proper amount of polyvinylpyrrolidone K30 and 0.01-0.05 part of magnesium stearate, wherein the brief molecular formula of the ganciclovir hydrate crystals is C9H13N504.1.5H2O; the weight of the ganciclovir hydrate crystals is calculated according to the weight of ganciclovir; and major peaks in powder XRD of the crystals are shown at diffraction angles of 5.45+/-0.1 degrees, 7.28+/-0.1 degrees, 11.45+/-0.1 degrees, 15.67+/-0.1 degrees and the like. The preparation technology of the prepared ganciclovir tablets is simple; tablets have good stability; dosage is accurate; active components are easy to dissolve; and the bioavailability of the active components is raised.
US20110117198 Compositions of semi-interpenetrating polymer network Novel compositions consisting of semi-interpenetrating network of cross-linked water soluble derivatives of basic polysaccharides and a non-cross-linked component, which is an anionic polysaccharide are provided. Methods for the production of such compositions are also disclosed. Preferably the basic polysaccharide is chitosan or a derivative thereof and the anionic polysaccharide is hyaluronic acid. The compositions can be formed into gels or films, for example, and thus find use in a wide range of medical applications in the fields of dermatology, plastic surgery, urology and orthopaedics.
US20100137448 Methods for Treating Neuropsychiatric Disorders with NMDA Receptor Antagonists The present invention relates to compositions and methods for treating a human patient afflicted with a neuropsychiatric disorder. Specifically, the invention provides for compositions and methods of modulating or antagonizing the activity of neuronal NMDA receptors, wherein such antagonistic activity is capable of modulating the glutamate induced excitatory response of the neurons, thereby inhibiting an excitotoxic effect, promoting a neurotrophic effect, and thereby providing a therapeutic effect that treats the neuropsychiatric disorder.
WO2012103037A1 Oil compositions The present invention provides oil compositions and associated methods and reagents, particularly useful for the treatment of dermatologic conditions. In some embodiments, provided compositions are formulated for and achieve transdermal delivery, for example by topical administration.
CN101773664B Fish bone scale collagen peptide for preventing and curing egg and poultry fracture The invention relates to fish bone scale collagen peptide for preventing and curing egg and poultry fracture, which comprises the following components in parts by weight: 10 to 300 of fish bone scale collagen peptide, 300 to 1000 of ginseng polysaccharide, and 1.5 to 30 of silymarin. The fish bone scale collagen peptide for preventing and curing egg and poultry fracture has the advantages of easyabsorption, good calcium supplementation effect and egg and poultry fracture prevention and curing effect.
CN103705447A Long-acting ceftiofur hydrochloride injection and preparation method thereof The invention relates to a long-acting ceftiofur hydrochloride injection. The injection is prepared by a method comprising the following steps: adding a ceftiofur hydrochloride ethanol solution into an ethyl beta-cyclodextrin saturated aqueous solution, stirring and including; filtering and sterilizing through a 0.22mu m milliporous filter membrane; performing spray drying to prepare a ceftiofur hydrochloride inclusion; adding a suspending agent, a dispersing agent and a stabilizing agent into partial injection solvent, dissolving at 100 DEG C, and adding the injection solvent to the whole amount, and performing dry heat sterilization at 150 DEG C for 1 hour; cooling the dispersion liquid to room temperature, adding the ceftiofur hydrochloride inclusion into the dispersion liquid, and uniformly stirring; adding the sterilized injection water, and uniformly stirring to obtain a mixed solution; preparing the long-acting ceftiofur hydrochloride injection by a high-speed shearing dispersion machine. The preparation process is simple in operation; the prepared suspension injection has the advantages of uniform granularity, good fluidity, slow settlement, good redispersion property, wall adhesion prevention of liquid medicine, good nozzle cleaning performance, no discoloration after long-term storage and stable chemical property. After the preparation is injected to a pig in an intramuscular manner, the preparation is released slowly, long in elimination half life, and smooth in plasma drug concentration, can be used for prolonging the effective acting period of the medicine in a body and reducing the number of administration times, and is convenient to use.
CN102151224A Infantile cerebral palsy acupuncture point heat treatment plaster The invention relates to an infantile cerebral palsy acupuncture point heat treatment plaster, which is a plaster for external use for treating infantile cerebral palsy. The infantile cerebral palsy acupuncture point heat treatment plaster consists of folium artemisiae argyi, lumbricus, Chinese angelica, kudzu root, nux vomica, storax, borneol, cinnamon, Kanlisha and magnetic treatment sheets, has the function of improving the brain tissue blood circulation and the brain tissue function, recovering brain lesion blood and oxygen supply, activating the damaged dormant brain tissue cells and vibrating and treating the palsy, has good treatment effect and quick return during the treatment of the infantile cerebral palsy, can achieve the effect of addressing both symptoms and root causes and the goal of not easily relapsing after recovery.
US20060073333 Dispersing a matrix of nanostructured liquid phase or a dehydrated variant and a nanostructured liquid crystalline phase or a dehydrated variant in nonlamellar material; cooling or evaporating a volatile solvent A particle coated with a nonlamellar material such as a nonlamellar crystalline material, a nonlamellar amorphous material, or a nonlamellar semi-crystalline material includes an internal matrix core having at least one a nanostructured liquid phase, or at least on nanostructured liquid crystalline phase or a combination of the two is used for the delivery of active agents such as pharmaceuticals, nutrients, pesticides, etc. The coated particle can be fabricated by a variety of different techniques where the exterior coating is a nonlaliellar material such as a nonlamellar crystalline material, a nonlamellar amorphous material, or a nonlamellar semi-crystalline material
CA2503183C Salmeterol superfine formulation The present invention relates to a pharmaceutical formulation for use in the administration of a long-acting .beta.2-agonist by inhalation. In particular this invention relates to a chemically stable, highly efficient salmeterol HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
US20120149657 2'-fluoro arabino nucleosides and use thereof A method of treating cancer using certain 2′-fluoro arabino nucleosides is provided. Also provided are compounds represented by the formula: (I & A) wherein R is alkyl; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions containing these compounds.
CN102391258A Amino-substituted flavone compound and preparation and use thereof The invention discloses an amino-substituted flavone compound or a pharmaceutically-acceptable salt and a preparation and use thereof. With the adoption of the amino-substituted flavone compound disclosed by the invention, the activity of a promoter for transcribing ABCA1 protein in macrophages of a mouse can be obviously enhanced, and then, the mRNA level and the protein level of the ABCA1 protein in the macrophages are increased. The increase of the expression of the ABCA1 protein in the macrophages has important significance on the prevention and the treatment of cardiovascular and cerebrovascular diseases caused by lipid metabolism disorders, such as arteriosclerosis, Alzheimer's disease and the like. The amino-substituted flavone compound has a structural formula shown as a formula (I) or a formula (II).
US20080234325 Novel Methods Using Pyridine Derivatives The invention provides methods of treating and preventing asthma, laryngitis, symptomatic gastroesophageal reflux disease, pregnancy-induced gastroesophageal reflux disease, noncardiac chest pains, coughing, apnea, dyspepsia, inflammatory bowel disease, irritable bowel syndrome, gastritis, stress ulcers, bleeding peptic ulcers, acute gastrointestinal bleeding, infectious enteritis, collagenous colitis, lymphocytic colitis, chronic diarrhea in immunocompromised patients, esophageal ulcers in immunocompromised patients, idiopathic gastric acid hypersecretion, gastroparesis, gastrointestinal motility disorders, Zollinger-Ellison syndrome, short bowel syndrome, emesis, regurgitation, early satiety, chronic sore throat, abdominal pain, abdominal bloating, nausea, sour stomach, diarrhea, constipation, bacterial infections, refractory ulcers, gastrointestinal disorders induced by NSAIDs, Barrett's esophagus, gastrointestinal disorders caused by steroids, gastrointestinal disorders induced by cholinergic compounds, and fungal or viral-induced ulcers in the gastrointestinal tract by administering a therapeutically effective amount of at least one of the pyridine derivatives of the invention to a patient in need thereof. The invention also provides on demand relief of symptoms associated with gastroesophageal reflux disease (GERD), and provides relief from symptoms caused by the consumption of excessive amounts of food and/or alcohol by administering a therapeutically effective amount of at least one of the pyridine derivatives of the invention to a patient in need thereof. The invention also provides methods for treating parasitic infections, such as malaria, by administering a therapeutically effective amount of at least one of the pyridine derivatives of the invention to a patient in need thereof. In preferred embodiments, the pyridine derivative of the invention is rabeprazole, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof.
EP1832657A1 Methylation of plasmid vectors The present invention provides a method of reducing a mammal's immunostimulatory response to a composition comprising the step of administering said composition wherein said composition comprises at least one plasmid, and at least one cationic amphiphile, wherein said at least one plasmid is a CpG altered plasmid and the method of altering said plasmid is chosen from removing at least one CpG motif from said plasmid, mehtylating at least one CpG motif of said plasmid, or removing at least one CpG motif and methylating at least one CpG motif.
US20070299068 viricides comprising (3-cyano-indol-2-yl)phenyl derivatives, used for for treating viral diseases and infections or for affecting viral internal ribosome entry site (IRES) activity The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.
US7300669 Fatty alcohol, skin conditioner, propylene glycol, mineral oil or white soft paraffin and water; fluticasone propionate and oil in water emulsion includig excipients; antiinflammatory agents A fluticasone lotion having improved vasoconstrictor and anti-inflammatory activity and higher than expected potency. The fluticasone lotion contains 0.05 weight percent fluticasone propionate and an oil-in-water vehicle that includes excipients. The fluticasone lotion is unexpectedly efficacious while exhibiting an improved safety profile.
CN101411699A Aceclofenac paracetamol tablet and preparation technique The invention discloses an aceclofenac paracetamol tablet, which uses aceclofenac and paracetamol as basic medicines, starch as a filling agent, hyprolose as a disintegrant, 20 percent polyvinyl pyrrolidone anhydrous ethyl alcohol solution as an adhesive, and magnesium stearate as a lubricant, and is prepared through pelletizing, drying, finishing granule, tabletting and lagging cover. Because the aceclofenac and the paracetamol are prepared into compound preparation, the aceclofenac paracetamol tablet has antipyretic, anti-inflammatory and analgesic efficacies, is suitable for the treatment of pain and inflammation symptoms caused by osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, lumbago, toothache and the like, and for the treatment of gynecological inflammation, and ear, nose and throat inflammations, and can be widely applied to the clinic.
EP2224933A2 Conjugated beta-1,3-linked glucans Glucans having exclusively or mainly β-1,3 linkages are used as immunogens. These comprise β-1,3-linked glucose residues. Optionally, they may include β-1,6-linked glucose residues, provided that the ratio of β-1,3-linked residues to β-1,6-linked residues is at least 8: 1 and/or there are one or more sequences of at least five adjacent non-terminal residues linked to other residues only by β-1,3 linkages. The glucans will usually be used in conjugated form. A preferred glucan source is curdlan, which may be hydrolysed to a suitable form prior to conjugation.
CN101049314A Dispersion tablet of asiaticoside and preparation method A dispersing tablet of asiaticoside is prepared from the asiaticoside and proper auxiliaries. Its preparing process is also disclosed.
US20110190225 Topical method for prompt relief of severe ascites A means is provided to make the capsules of cirrhotic or fibrotic livers relatively impermeable to liver tissue fluid or lymph in humans or other mammals suffering from severe chronic ascites or refractory ascites by application of collodion. The means will be useful to decrease the need for liver and combined liver and kidney transplantations
CN102670495A Azasetron hydrochloride injection and preparation method thereof The invention discloses azasetron hydrochloride injection and a preparation method thereof. The injection contains the following components in parts by mass: 10 parts of azasetron hydrochloride, 10 to 20 parts of L-arginine, 16 to 20 parts of sodium chloride and 1.6 to 3.0 parts of lactic acid. The injection is prepared by the following steps of: adding injection water into a proportioning tank, adding sodium chloride, lactic acid, L-arginine and azasetron hydrochloride in a formula amount, stirring for dissolving, regulating the pH to be 3.8-4.2, keeping the temperature of medicinal liquid between 50 and 60 DEG C, performing heat preservation adsorption by using active carbon, setting the volume, de-carbonizing, filtering, cooling to room temperature, performing fine filtration, charging nitrogen, and filling. The injection is high in stability, and has a remarkable effect of inhibiting vomit.
EP2097402A1 Macrocyclic inhibitors of hepatitis c virus Inhibitors of HCV replication of Formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is -OR7, -NH-SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1 -6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1 -6alkyl, C3 -7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1 -6alkoxy, polyhaloC1 -6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1 -6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally co mprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally subst ituted with C1-6alkyl; or C1-6alkyl optionally subst ituted with C3 -7cycloalkyl; R8 is C3-7cycloalkyl optionally subst ituted with C1 -6alkyl; C1 -6alkyl optionally substituted with C3-7cycloalkyl; or -NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturated heterocyclic ring; pharmaceut ical compositions containing compounds (I) and processes for preparing compounds (I).
WO2008041843A1 Inhibition of cholera toxins by galatooligosaccharides (gos) The invention relates to nutritional and pharmaceutical compositions comprising non-digestible galactooligosaccharides (GOS) and uses thereof. In particular, it relates to the use of GOS species in preventing or treating disease caused by bacterial toxins. Provided is the use of GOS having a polymerization degree of 5 or higher, preferably 6 or higher, for the manufacture of a nutritional or pharmaceutical composition for the treatment or prevention of an acute or chronic disease associated with or caused by the adhesion and/or uptake of a cholera toxin family member. Also provided is a method for providing a GOS fraction capable of inhibiting cholera toxin (Ctx) binding to GMl and fractions obtainable thereby.
CN1634038A Anethol trithione soft capsule and its preparation method The invention relates to an anethol trithione soft capsule and its preparation method, wherein the soft capsule comprises soup and capsule casing, the soup contains medicinal active agent of anethol trithione and medicinal adjuvant, while the medicinal findings include diluent, anti-oxidant agent, suspension adjuvant and emulsifying agent. The invention has the advantages of high biological availability, good packing property and accurate content.
US20090270498 Lipoxin Compounds and Their use in Treating Cell Proliferative Disorders Compounds having the active site of natural lipoxins, but a longer tissue half-life are disclosed. In particular, 15-epi-lipoxins and their use in ameliorating undesired cell proliferation, which characterizes diseases such as cancer, are also disclosed.
US8273381 Compositions for and methods of controlling olfactory responses to odorants A composition, system and method for modifying an olfactory response to an odorant is disclosed. In some embodiments, the composition includes crystalline metal nanoparticles dispersed in an aqueous medium. The composition is applied to olfactory tissues using a suitable applicator or dispenser. The metal nanoparticles are believed to interact with a G-protein coupled to receptor located in the cilia to moderate (enhance or reduce) sensitivity or ability to smell particular odorants. In accordance with an embodiment of the invention, the composition includes one or more odorants.
CA2334773C Benzothiepine-1,1-dioxide derivatives, method for producing them, medicaments containing these compounds and their use The invention relates to benzothiepine-1,1-dioxide derivatives and their acid addition salts, i.e. compounds of formula (I) wherein R1, R2, R3, R4, R5 and Z have the meanings given in the description and their physiologically compatible salts and physiologically functional derivatives. The invention also relates to a method for producing said compounds, which are suitable for use as e.g. hypolipidaemics.
CN101475575B Extraction of tetraodontoxin, and preparation thereof used in drug dependence of dolantin The invention relates to the extraction of tetraodontoxin and a preparation of the same. The extraction of the tetraodontoxin comprises: a fist step of extracting a stock solution, in which ovaries of Takifugu flavidus are soaked in an HAC solution to form the stock solution; a second step of resin exchange, in which resin which is D152 positive macroporous weakly acidic acrylic resin is converted to NH4 type by a conventional method, two columns carry out resin exchange for two times, a lower layer of the inside of the A column which is a glass column contains resin, an upper layer of the the inside of the A column contains diatomaceous earth, a lower layer of the inside of the B which is a glass column contains neutral alumina, an upper layer of the inside of the B column contains resin; and a third step of elution carried out after exchange of the two columns, in which strong toxins collected after exchanged and elution are mixed after the elution of the two columns and a coarse product of tetraodontoxin is obtained by crystallization. The method for extracting the tetraodontoxin improves the product yield and purity. The preparation has the characteristics of longer storage period, and quick effect, complete control over symptoms, smooth transition, easy reception and the like in use for de-addiction treatment.
CN103298819A Crystalline 6,7-unsaturated-7-carbamoyl morphinane derivative, and method for producing same The present invention provides a compound represented by Formula (IA): an acid addition salt thereof, and/or stable crystals of solvates thereof. The crystals are extremely useful as an active ingredient for producing pharmaceutical products. The present invention further provides a novel method for producing a 6,7-unsaturated-7-carbamoyl morphinane derivative.
DE102007054877A1 Use of hyaluronidase e.g. as a drug for the treatment of profibrotic metabolic disorder, fibrotic liver disease, chronic viral liver disease, portal hypertension, chronic hepatitis C and hepatocellular carcinoma Use of hyaluronidase (I) as a drug for the treatment of liver disease with profibrotic metabolic disorder, is claimed. - ACTIVITY : Hepatotropic; Cerebroprotective; Hypotensive; Cytostatic; Antiinflammatory; Virucide; Metabolic. - MECHANISM OF ACTION : None given.
US20110218192 Inhibitors Of Beta-Secretase The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
EP2573079A2 Benzimidazole quinolinones and uses thereof Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
CN1660117A Application of diltiazem of hydrochloric acid in preparing antidote An application of diltiazem hydrochloride in preparing the detoxicant for treating the CCl4 poisoned hepatitis and cocaine poisoned hepatitis is disclosed.
US20120071509 process The present invention relates to improved processes for preparing 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (I) (lenalidomide) and its intermediate 3-(1-oxo-4-nitro-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to improved processes for preparing lenalidomide crystalline form A, use of said crystalline form A as an active pharmaceutical ingredient or as an intermediate in the preparation of further crystalline or amorphous forms of lenalidomide, compositions comprising lenalidomide crystalline form A and their use in the treatment of disease.
EP1855670A2 Benzazole potentiators of metabotropic glutamate receptors The present invention is directed to benzazole compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
CN103006547A Dolasetron mesylate containing injection, as well as preparation method and quality control method thereof The invention provides a dolasetron mesylate containing injection. The injection comprises dolasetron mesylate, a polyhydroxy compound, a pH regulator and pharmaceutically acceptable auxiliary materials, wherein the polyhydroxy compound serving as a stabilizing agent is one or more of mannitol, xylitol and sorbitol; the pH regulator is one or more of hydrochloric acid, sulfuric acid, phosphoric acid, citric acid, acetic acid, maleic acid, tartaric acid and lactic acid, and the pH value of the injection can be kept in an acceptable range. The invention also provides a preparation method and quality control method of the injection.
WO2008015202A3 Anticonvulsive pharmaceutical compositions The present invention pertains to pharmaceutical compositions comprising, as the active ingredients, a combination of vigabatrin and of at least one substance having anti-ischemic effect.
EP0804438B1 Tricyclic benzazepine vasopressin antagonists Tricyclic compound of general formula (I) as defined herein which exhibit antagonist activity at V1 and/or V2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.
WO2006052913A1 PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES The present invention relates to compounds of formula (I) useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention.
CN101401783A Percutaneous absorption agent containing Ailamode, preparation method and medical uses thereof The invention relates to a transdermal absorbent containing Iguratimod, which comprises gellies, ointment, and cream, wherein the mass percentage content of the Iguratimod in the transdermal absorbent is between 0.1 and 10 percent, and preferably the mass percentage content of the Iguratimod in the transdermal absorbent is between 0.4 and 3 percent; and the invention also discloses requirements of the transdermal absorbent on the selections of matrix and a transdermal enhancer. Furthermore, the invention also provides a method for preparing the transdermal absorbent containing the Iguratimod and pharmaceutical application thereof.
CN103301462A Component and method for treating virus disease The invention relates to a component and a method for treating a virus disease, and firstly discloses a novel application of a P2X receptor antagonist in preparing a composition for treating the virus infection disease. The P2X receptor antagonist is used for preventing or treating a hand-foot-and-mouth disease by suppressing the virus exertion.
EP2081951A1 Progesterone receptor antagonists The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.
CN101209086A Mineral substance type salt for dairy cattle and manufacturing method thereof A mineral salt for dairy cattle is characterized in that the main component of the salt includes sodium chloride, organic chrome, mineral salt, nonprotein nitrogen, flavouring agent and jointing compound. A manufacturing method of the mineral salt includes: (1) weighing; (2) pretreating the materials; (3) mixing and stirring; (4) feeding mold; (5) pressing to form; (6) storing; (7) checking product; (8) packaging, namely finished product. The invention has the advantages of : (1) abundant nutrition, having the remarkable effects of improving the immunity and increasing milk and being able to complement the insufficiency of the protein supplied in the feed, good taste; (2) scientifically and reasonably selection on the adding mode of each component of the mineral and microelement; (3) easy material acquirement and low manufacture cost; (4) effectively improving the uniformity of the material mixing and shortening the mixing time by the measures of pretreating and mixing, not exceeding 5 percent on the uniformity of the material which is better than the standard that the international standard of uniformity is less than 10 percent; (5) adopting a press forming method and being safe, saving energy and protecting environment in the manufacturing method; (6) increasing the variety of salt products and improving the economic benefits of enterprises.
CN101507705A Preparation method of block polymer micelle administration system with targeting effect The invention relates to a method for preparing a block polymer micelle drug delivery system with the targeting in the technical field of medicine. The method comprises the steps of: utilizing a carboxylated PEO-PPO-PEO block polymer as a carrier to construct a micellar water solution of an insoluble drug, activating carboxyl groups of PEO-PPO-PEO by a carboxyl activating agent to prepare a PEO-PPO-PEO drug delivery micelle system connected with targeting molecules such as related ligands or antibodies and the like, and obtaining a lyophilized preparation of the targeted drug delivery micelle system after bacteria removal by filtration and freeze drying. The method has the advantages of simple operation, mild conditions, cheap raw materials, no need of adopting a composite material, and strong controllability, can realize the active targeting effect on the premise of maintaining the characteristics of PEO-PPO-PEO drug delivery micelles such as small particle size, no immunogenicity and the like, reduce the damage of therapeutic drugs to surrounding normal tissue cells, reduce toxic side effect and drug dosage, and is suitable for mass preparation and industrial production.
CN101428031A Medicament preparation for preventing cardiovascular diseases The invention discloses pharmaceutical preparation for preventing cardiovascular and cerebrovascular diseases. The pharmaceutical preparation is compound preparation which comprises aspirin and misoprostol; the dosage form of the compound preparation is pharmaceutical tablets, double-layer tablets or capsules which comprise aspirin and misoprostol. The preparation method of the pharmaceutical preparation comprises the following steps: preparing aspirin and misoprostol into micropills, and then preparing into tablets or capsules for taking. The drug is distributed uniformly in the gastrointestinal tracts, and belongs to a multi-unit administration system, the transport of the drug in the gastrointestinal tracts is hardly influenced by the food conveying rhythm, the difference of the drug in an individual and among individuals is small, the compliance of the patient is good, stimulation and untoward reaction which are caused by too high medicine concentration in local parts can be reduced, and injury of aspirin to the gastrointestinal tracts can be reduced or avoided; in the production process, the grain size of the two medicines is similar, and the misoprostol micropills are easy to uniformly blend with other micropills, so that the quality of the medicine is improved; the common tabletting technique and auxiliary material tabletting can be used, so as to reduce the production cost of the medicine.
CA2724023C Salicylate conjugates useful for treating metabolic disorders The present invention is directed to methods for treating metabolic disorders with compounds that are salicylate conjugates.
CA2271268C Therapeutic and cosmetic compositions comprising an extract of crude shark liver oil, their use and method for the preparation thereof A composition comprising as active ingredients (i) one or several components derived from an extract of crude shark liver oil, selected from the group comprising refined shark liver oil or a fraction thereof, squalane, squalene and alkylglycerols, and/or the synthetic equivalents of these; (ii) one or several carbohydrates forming inclusion and/or chelate complex with (i); and optionally (iii) one or several non-shark liver oil derived therapeutically or cosmetically active agents. A method of preparing the composition, as well as the use of the composition for the preparation of a pharmaceutical or cosmetic.
EP1578416B1 Medicaments containing substituted 2,5-diaminomethyl-1h-pyrroles The invention relates to medicaments containing substituted 2,5-diaminomethyl-1H-pyrroles and the use of said compounds for producing medicaments.
EP1380295B1 Photosensitiser and method for production thereof The invention relates to medicine and concerns a photosensitiser for detecting and curing tumors. The inventive photosensitiser is embodied in the form of a composition containing chlorine in the form of salt and alkali metals. 80-90% of chlorine e6, 5-20% of purpurin 5 and the rest being purpurin 18 are used as chlorine. Said photosensitiser is produced by extracting Spirulina biomass with the aid of aceton. Afterwards said biomass is exposed to acid treatment, neutralisation, hydrolysis, extraction of feoforbide α, dissolution in aceton, addition of a strong base, neutralisation and reprecipitation of chlorine 6.
CN201515743U Sterilization sweat absorbing massage magnetic treatment insole The utility model relates to an insole which is suitable for various leather shoes, fabric shoes, cotton padded shoes, sports shoes and hiking shoe, wherein a sterilization sweat absorbing massage magnetic treatment insole comprises an insole liner and medicine positioned in the insole liner. The sterilization sweat absorbing massage magnetic treatment insole is characterized in that a permanent magnetizing ball is arranged in the insole liner, and the insole liner is sleeved by an insole coat. The insole has the functions of heat reduction, sweat absorption and fungus and inhibition to calced feet, and the insole also has the human sole massage and magnet treatment functions and health-care effect.
EP2349250A1 Fatty acids for use as a medicament The invention relates to fatty acid stimulation of rectal mucosa initiating the process of defecation, acting as a laxative. Furthermore, the invention relates to the usage of free fatty acids, fatty acid mixtures and fatty acid extracts from marine lipids in pharmaceutical formulations such as suppositories, ointments, tablets and gelatin capsules for treatment and prevention of multiple disorders like constipation, hemorrhoids, bacterial infections (e.g. helicobacter pylori), viral infections (e.g. herpes simplex virus infections) and inflammations, as well as against fissura ani and pruritus ani.
EP2415767A1 Poly (ADP-ribose) Polymerase (PARP) Inhibitors The invention provides compounds of the general formula (1): wherein the variables are as defined herein. The compounds have use in inhibiting poly (ADP-ribose) Polymerase (PARP). The invention also provides pharmaceutical compositions containing the compounds and their use as medicaments.
WO2009158381A1 Novel psymberin derivatives, compositions, and their use as antineoplastic agents The present invention provides compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers thereof, wherein: ring A, n, q, R1, R2, R3, R4, R5, R6, each R7, each R7A, and R8 are each selected independently of each other and as defined herein. The invention also provides pharmaceutical compositions comprising such compounds (optionally in combination with one or more additional active ingredients), and methods for their use in treating or preventing a wide range of cancers.
WO2014059884A1 Marker of metabolite of optically-active 2-hydroxyltetrathienopyridine derivative, and preparation method and use thereof The present invention relates to the field of medicine, and in particular, to a new marker of a metabolite and pharmaceutical use thereof in studying or preparing a medicine comprising optically-active 2-hydroxyltetrathienopyridine derivatives, and the medicine can be used for preventing or healing diseases caused by thrombus. The present invention further provides a preparation method of the new marker of the metabolite.
WO2011033884A1 Prophylactic agent for muscular contracture A pharmaceutical material or a food material which contains a caroteine oxidation derivative derived from a land animal, a land plant or a microorganism as an active ingredient, is suitable for use in a food, a beverage or a drug, and can ameliorate muscle tonus, alleviate muscular fatigue, or prevent muscular contracture.
CN101780030A Ginkgo flavone aglycone solid dispersion and preparation method thereof The invention relates to a ginkgo flavone aglycone solid dispersion and a preparation method thereof. The solid dispersion adopts ginkgo flavone aglycone as active ingredient, is added with polymer carrier material, antioxidant and antisticking agent according to the proportion of 1: (0.2-15): (0-5): (0.2-15), and is prepared by a melting method, a coprecipitation method, a solvent dispersion method, a solvent melting method or a grinding method. The polymer carrier material is one or more in povidones, polyethylene glycols, poloxamers, polyoxyethylene stearic acid, hydroxymethyl propyl celluloses and low-viscosity Eudragit; the antioxidant is one or more in vitamin E, vitamin C or edetate disodium; the antisticking agent is one or more in talcum powder, micropowder silica gel, magnesium stearate or other auxiliary materials which can be taken as the antisticking agents. The ginkgo flavone aglycone solid dispersion can improve the solubility of medicine, leads the solubility to be 5-500 times higher than that of raw medicine, accelerates the dissolution rate of the medicine, and remarkably improves the dissolution rate in a dissolution medium within 45min in an accumulated way.
CA2856403A1 Pharmaceutical compositions comprising deuterium-enriched perillyl alcohol, iso-perillyl alcohol and derivatives thereof The present invention, provides for a deuterium-enriched monoterpene or sesquiterpene such as perillyl alcohol, or a deuterium-enriched isomer or analog of monoterpenes or sesquiterpenes, such as isoperillyl alcohol. The present invention also provides for a deuterium-enriched derivative of a monoterpene or sesquiterpene, such as a perillyl alcohol carbamate, or a deuterium-enriched derivative of an isomer or analog of a monoterpene or sesquiterpene, such as an isoperillyl alcohol carbamate. The deuterium-enriched derivative may be perillyl alcohol or isoperillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a deuterium-enriched compound.
US20110092593 Water-Soluble Colonoscopy Lubricant Disclosed is a water-soluble colonoscopy lubricant essentially comprising Polyethylene Glycol 400; Propylene Glycol; and Glycerin. Distilled water may be added as needed to achieve a desired viscosity. Additional ingredients such as a preservative and a pH adjuster may also be added to the colonoscopy lubricant.
DE102006021198A1 Concentrated aqueous solution of sodium chloride in combination with concentrated aqueous solution of sodium chloride with UV-A light or UV-B light for dermal application against skin disease (pigment disorder), preferably vitiligo Concentrated aqueous solution of sodium chloride (salt solution) in combination with concentrated aqueous solution of sodium chloride (salt solution) with UV-A light (320-400 nm) and/or UV-B light (290-320 nm) for dermal application against the skin disease (pigment disorder) vitiligo, where the aqueous sodium chloride solution exhibits a concentration of 0.1 molar solution up to a saturated approximately 6.7 molar solution. - ACTIVITY : Dermatological. - MECHANISM OF ACTION : None given.
EP2034015A1 Immunostimulatory oligonucleotide and pharmaceutical application thereof A novel immunostimulatory oligonucleotide by which an IFN-inducing activity is enhanced and an inflammatory cytokine-inducing activity is reduced, and a pharmaceutical containing the same, and an aplication thereof are provided. That is, the present invention provides the immunostimulatory oligonucleotide composed of a base sequence represented by a formula: 5'-(G)MPXCGYQ(G)N-3' (X and Y are mutually independent and represent an arbitrary sequence which has a length of 0 to 10 nucleotides and does not contain 4 or more consecutive G residues, and a length of X + Y is 6 to 20 nucleotides; XCGY contains a palindrome sequence having a length of at least 8 nucleotides and has a length of 8 to 22 nucleotides; P and Q are mutually independent and represent one nucleotide other than G; M represents an integer of 6 to 10 and N represents an integer of 0 to 3) wherein a full length thereof is 16 to 37 nucleotides (except for an oligonucleotide composed of a basesequence represented by SEQ ID NO:5), the pharmaceutical application thereof.
WO2011045803A1 Sore relief formulation The present invention relates to sore relief formulations containing calamine, zinc oxide and boric acid as well as a method for preparing the same.
WO2008035982B1 COMBINATION OF A GLUCOCORTICOID AND A β-CYCLODEXTRIN CONJUGATED VITAMIN A DERIVATE COMPLEX The present invention is related to a pharmaceutical combination of a glucocorticoid and a β-cyclodextrin conjugated vitamin A derivative complex as well as a pharmaceutical composition comprising the same. The combination and the composition of the invention can be used for reducing or eliminating skin atrophy induced by treatment with glucocorticoids (GC). Also comprised is a method for reducing or eliminating skin atrophy induced by GC treatment. Furthermore the invention concerns a kit comprising a glucocorticoid and a β-cyclodextrin conjugated vitamin A derivative complex.
CN102698008A Preparation technique for yuyeyuan integrated new dosage form and production method thereof The present invention relates to a preparation technique for a yuyeyuan integrated new dosage form and a production method thereof. Raw material composition of effective components by weight ratio is 30 parts of gypsum rubrum, 10 parts of alum, and 10 parts of pinellia ternata. The production processes include: supersonic air jet pulverization, alcohol and water extraction, ultrasonic pulverizing extraction, concentrated decoction, supersonic spray drying, nano-grinding, high-pressure homogenization, and nanoparticle preparation. The invention emphasizes the utilization of the advantages of multi-collaboration and multi-targets embodied in nanocarrier combination technology. The technique can significantly reduce production costs, significantly improve the quality of products, and enhance targeting and controlled-release of the yuyeyuan after scale production. The yuyeyuan can be dosed inside and outside simultaneously, and can be respectively taken at four time periods according to midnight-midday ebb flow and human qi and blood flow law. The yuyeyuan can also be prepared into a film agent and a transdermal agent according to the midnight-midday ebb flow and the human qi and blood flow law to be respectively attached on different parts of a human body, and can be directly absorbed through the skin.
US20120195906 Method for diagnosing and treating emphysema The present invention provides methods for diagnosing a patient with emphysema or COPD by detecting the levels of EMAP II in a sample. Alternatively, methods are provided for determining the susceptibility of a patient to develop emphysema or COPD by detecting the levels of EMAP II in a sample. The levels of EMAP II may be determined by immunoassay techniques. The present invention also provides methods for treating patients with emphysema or COPD by administering a therapeutically effective amount of an EMAP II neutralizing compound. The compound may be an antibody, siRNA, antisense RNA or an antagonist of CXCR3.
US20090274778 Compositions Exhibiting Inhibition Of Cyclooxygenase-2 The invention provides a method of treating diabetes by administering to an individual having diabetes a composition containing a hops extract. In a particular embodiment, an individual having diabetes can be administered a composition comprising a first component selected from the group consisting of alpha acids and beta acids, essential oils, fats and waxed, with the proviso that the first component and second component are not the same compound. The invention additional provides a method of treating diabetes by administering to an individual having diabetes a composition comprising a first component selected from a curcuminoid and a second component selected from an alpha acid and a beta acid.
EP2151237A1 Pharmaceutical composition combining a non-steroidal anti-inflammatory agent and an anticonvulsant agent The invention relates to a pharmaceutical composition comprising a synergic combination of an anticonvulsant agent such as the active principle: gabapentin and a non-steroidal anti-inflammatory agent such as the active principle: meloxicam, which are formulated in a single dosage unit for oral administration, said composition being intended for the treatment of neuropathic pain caused by different etiologies.
CN103130854A Vitamin E succinic acid esterification gemcitabine prodrug and application The invention discloses a vitamin E succinic acid esterification gemcitabine prodrug which is characterized in that vitamin E succinic acid ester is connected with N4-amino of gemcitabine through an amido bond and the vitamin E succinic acid esterification gemcitabine prodrug has the following formula structure. By means of the vitamin E succinic acid esterification gemcitabine prodrug, the defect that gemcitabine (dFdC) is fast in metabolism is overcome, cycling time of the dFdC is a human body is prolonged, the mode in which the dFdC entering a cell is changed, namely the dFdC no longer enters into the cell relying on a nucleoside transport protein carrier, thus generation of drug resistance is avoided, meanwhile toxic and side effects of the dFdC are reduced furthest, curative effects and bioavailability are improved notably, and the bottleneck that the clinical effect of the dFdC on pancreatic is non-ideal at present is broken.
WO2006003518A3 6-phosphorylcholine-n-acetyl-d-galactosamine conjugate molecules and their use in vaccinal, therapeutic and diagnostic applications against bacterial infection of the respiratory tract The present invention relates to carbohydrate-phosphorylcholine conjugate molecule, and more particularly to phosphorylcholine-N-acetyl-D-galactosamine molecules and their use for treating and/or preventing a bacterial infection of the respiratory tract. More specifically, in this present application, the inventors aimed at raising high-affinity antibodies against ChoP preferably in its bacterial context in order to target several pathogens of the respiratory tract. By mimicking the S. pneumoniae model, the inventors preferably synthesized two carbohydrate-ChoP (GalNAc-ChoP) protein conjugates and showed that these immunogens induce hapten-specific antibodies which recognize two major bacterial pathogens of the respiratory tract : such as a Gram-positive bacterium, S. pneumoniae, and a Gram-negative bacterium, N. meningitidis.
WO2006106711A1 Antifungal agent containing pyridine derivative It is intended to provide an antifungal agent which has an excellent antifungal effect and is also excellent in physical properties, safety and metabolic stability. Namely, a compound represented by the following general formula and an antifungal agent containing this compound: (I) wherein X represents oxygen, sulfur or -NH-; R1 represents hydrogen, halogen, cyano, amino or a substituent; and R2 and R3 independently represent each hydrogen, halogen, hydroxyl or a substituent, excluding the case where R2 and R3 are both hydrogen atoms.
CN1602877A Pharmaceutical composition for treating somatization disorder and its preparation process The invention discloses a drug combination for curing body form obstruction and its preparing method, mainly containing the following components in weight shares: penfluridol 1-3, sulpiride 90-110, and clonazepam 0.3-0.5. It is prepared in extremely low dosage and its action character: stopping the activation action of reticulate esoderma system of the brain to eliminate multiple symptoms of dysphrenia. And it has advantages of remarkable curative effect, small toxic and side effect, short period of treatment, low curing expenses, and being easy to take.
CN101780065A Application of calcium disodium edetate in preparation of medicine for inhibiting connective tissue growth factor and monoamine oxidase of human beings and mammal The invention relates to the application of calcium disodium edetate in the preparation of medicine for inhibiting connective tissue growth factor and monoamine oxidase of human beings and mammal; the calcium disodium edetate is injection when being applied to prepare the medicine of the diseases, and the injection contains 5-30wt % of calcium disodium edetate and auxiliary material used for the injection; the preferable lung target injection contains 0.1-5wt% of calcium disodium edetate and one or more auxiliary material(s) which is/are applicable to lung target preparation; the lung target injection is microsphere preparation, microcapsule preparation or liposome injection; preferably, the particle sizes of microspheres, microcapsules and liposome are 7-30 mu m; and the lung target preparation is preferably liposome injection liquid.
EP2542059A1 Compositions comprising myristic acid and uses thereof The teachings herein are directed to antibacterial and anti-inflammatory pharmaceutical compositions that include myristic acid. Further embodiments herein are directed to methods of administering sufficient amounts of myristic compositions to patients in need thereof in order to prevent or treat inflammation and/or bacterial infection. Myristic acid has been established to outperform other cetylated fatty acids in treating infection and inflammation, such as 1-TDC which includes cetylated myristic acid. The compositions and methods provided herein can further be used with additional anti-inflammatory, antibacterial, and delivery agents.
US20060199865 Synergistic combination comprising roflumilast and (r,r) - formoterol The invention relates to the combined administration of roflumilast and R,R-formoterol for the treatment of respiratory tract disorders.
CA2759936A1 Oral compositions for skin benefits Oral compositions containing a combination of antioxidants consisting of a water soluble vitamin, a water insoluble vitamin, a tea extract and gallic acid are used to maintain a beneficial amount of such antioxidants in a consumers bloodstream for maintenance and protection of healthy skin. The unique combination of ingredients provides a decrease in oxidative stress when exposed to UVB radiation, thereby promoting healthy skin.
CN103191055A Preparation method of orbifloxacin injection The invention relates to a preparation method of an orbifloxacin injection. The preparation method comprises the following steps of: putting orbifloxacin into injection water so as to obtain orbifloxacin suspension, adding a medical available acid which can dissolve orbifloxacin into the orbifloxacin suspension so as to obtain an orbifloxacin salt solution, filtering, concentrating and crystallizing so as to obtain solid orbifloxacin salt, subsequently adding an isosmotic adjusting agent, furthermore conditioning the pH value to be 3.5-4.5 by using an acid conditioning agent, diluting the solution by using injection water till the content of orbifloxacin in the solution is 2-100mg/ml, sterilizing, filtering, filling into bottles, charging an inert gas, namely, nitrogen, into the bottles to replace the air in the bottles, and sealing so as to obtain the orbifloxacin injection. The preparation method has the advantages that the prepared orbifloxacin injection can be directly injected into animals in sick in an injection mode, so that the blood concentration of orbifloxacin is rapid to achieve the peak, and the treatment on critical animals in sick is facilitated.
EP1492541A1 Pharmaceutical compositions comprising a 11-beta hydroxysteroid dehydrogenase inhibitor and a diuretic agent We provide a composition comprising a first agent which is an antagonist of 11β-HSD1, together with a second agent comprising a diuretic. The second agent may comprise a molecule which is capable of modulating an interaction between the first agent and 11β-HSD2. Such a composition may be used for improving cognitive ability of an individual, specifically verbal fluency or verbal memory or logical memory (or any combination thereof), or for treatment of Mild Cognitive Impairment (MCI).
US20080058396 Administering bryostatins as activators and Protein Kinase C, for stimulation of dendritic spine density The present invention provides methods of slowing or reversing the loss of memory and learning comprising the steps of contacting an effective amount of a PKC activator with a protein kinase C (PKC) in a subject identified with memory loss slowing or reversing memory loss. The present invention provides methods of stimulating cellular growth, neuronal growth, dendritic growth, dendritic spine formation, dendritic spine density, and the translocation of ELAV to proximal dendrites, and synaptic remodeling. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.
US20110092547 Chemical compounds 979 Compounds of formula (I), or pharmaceutically-acceptable salts and/or pro-drugs thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein n is 0 to 3; p is 0 or 1; q is 0 to 2; R1 and R2 are, for example, independently fluoro, chloro, bromo, cyano or (1-4C)alkyl; X is —O—, —S— or —NRa— wherein Ra is hydrogen or (1-4C)alkyl; RA1 and RA2 are, for example, independently hydrogen or (1-4C)alkyl; Ring A is a di-linked ring or ring system chosen from (4-6C)cycloalkane, (7-10C)bicycloalkane and (8-12C)tricycloalkane each optionally substituted, for example, by one substituent selected from (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; or Ring A is phenylene optionally substituted, for example, by up to four substituents selected from fluoro, chloro, bromo, cyano, (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
WO2005025571A1 A pharmaceutical composition comprising a p2x7 receptor antagonist and a nonsteroidal anti inflammatory drug. The invention provides a pharmaceutical composition, pharmaceutical product or kit comprising a first active ingredient which is a P2X7 receptor antagonist, and a second active ingredient which is a nonsteroidal anti-inflammatory drug, for use in the treatment of inflammatory disorders.
WO2013117008A1 Composition comprising hawthorn and phytosterols The composition comprising hawthorn and phytosterols for use in the treatment, alleviation or prevention of disorders associated with hypercholesterolemia and/or hyperlipidemia is described.
CA2516745A1 Botulinum toxin in treatment of clubfoot relapse Botulinum toxin, or other neuromuscular inhibitors, injected into the lower leg muscle of infants, less than a year old, with idiopathic clubfoot is shown to be an effective therapy in correcting this physical deformity. Following a protocol of manipulations, castings, and injections, clubfoot is effectively treated, and surgical treatment procedures can be avoided.
CN101067004A Moxa leaf polysaccharide and its use The present invention discloses moxa leaf polysaccharide and its use. The compound has obvious tumor inhibiting effect, capacity of enhancing body's immunological function and powerful antioxidation effect, and may be used for the auxiliary treatment of tumor and taken by persons with weak health. It has reliable curative effect, low cost and no toxic side effect.
WO2007068815A3 Heterocyclic derivatives, preparation and therapeutic use thereof The invention concerns compounds of formula (I) wherein: X represents a -C-, -SO2-, -C-N(R5)-C-N(R5)- group; Y represents an oxygen atom or a sulphur atom; R1 represents a hydrogen atom or a C1-C4 alkyl group; R2 represents a C1-C7 alkyl group, a carbocyclic radical, a methyl substituted by a C3-C12 non aromatic carbocyclic radical, a phenyl, a phenoxymethyl, a benzyl, a benzhydryl, a benzhydrylmethyl group, a 1,2,3,4-tetrahydronaphthalenyl, a pyrrolyl, imidazolyl, pyridyl, pyrazolyl, furyl, thienyl radical; an indolyl; a benzofuryl; R3 represents a substituted or unsubstituted phenyl; R4 represents a substituted or unsubstituted phenyl; R5 represents a hydrogen atom or a C1-C4 alkyl; as well as their salts and solvates. The invention also concerns a method for preparing same and the therapeutic use thereof.
CN1989962B Capsule comprising moguisteine The invention provides a Moggi Stan capsules, its characteristics are: mixing Moggi Stan and hydrophilic substances, disintegrating or abrading together, then mixing them with other excipients, filling capsules after preparing tablets with whole powder method or dry method. It has effects of moisture proof, avoiding light and so on, and can conceal adverse tastes of drug, but also avoids the maindrug melting in wet method preparing tablets heating process, while ensures rapid drug absorption and dissolution.
CN102190633A Cetirizine derivatives, and composition and application thereof The invention discloses cetirizine derivatives disclosed as a general formula 1, and a preparation method thereof. The compounds have greatly higher efficiency of passing through biomembranes, and have antihistamine activity in vivo after percutaneous absorption. The invention also relates to a pharmaceutical composition comprising the compounds, and application of the compounds in preparation of medicaments for treating allergic diseases. General formula 1.
US20080267903 Cationic polyamines and dendrimeric polymers; anti-proliferative agents; for treatment of neoplasms and tumours, inflammatory disorders, autoimmune disorders, psoriasis, and atherosclerosis; gene therapy Various polymers, including cationic polyamine polymers and dendrimeric polymers, are shown to possess anti-proliferative activity, and may therefore be useful for treatment of disorders characterised by undesirable cellular proliferation such as neoplasms and tumours, inflammatory disorders (including autoimmune disorders), psoriasis and atherosclerosis. The polymers may be used alone as active agents, or as delivery vehicles for other therapeutic agents, such as drug molecules or nucleic acids for gene therapy. In such cases, the polymers' own intrinsic anti-tumour activity may complement the activity of the agent to be delivered.
US20120141602 Systems containing magnetic nanoparticles and polymers, such as nanocomposites and ferrofluids, and applications thereof The present invention relates to a system comprising magnetic nanoparticles of a metal oxide and a polymer, which in turn contains monomers with different functional groups. This system can be solid (nanocomposite) or liquid (ferrofluid). The present invention also relates to a process for obtaining the system, as well as its use, mainly in biotechnological, veterinary and medical applications, such as, for example, for the diagnosis and treatment of human diseases.
US7037904 Improved appetite and energy level; reduced nausea and vomiting; immunostimulation; sleep and emotional support The present invention has disclosed a use of N-acetyl-D-glucosamine in the manufacture of a medicament for inhibiting the side effect of radio-chemical therapy, the medicament with N-acetyl-D-glucosamine as main active component can be used to inhibit the side effect of radio-chemical therapy of cancer patients, with an effective rate up to 85%.
US20090192153 Novel adenine compound An adenine compound or its pharmaceutically acceptable salt as a medicament as shown following formula (1): wherein R1 is optionally substituted alkyl group, etc., X is oxygen atom, etc., A is 4 to 8 membered optionally substituted saturated or unsaturated heterocyclic group containing 1 to 2 hetero atoms selected from 1 to 3 nitrogen atoms, 0 to 1 oxygen atom and 0 to 1 sulfur atom, L1 and L2 are independently straight or branched chain alkylene, or a single bond, R2 is optionally substituted alkyl group, etc.
WO2006000158A8 The use of laetispicine for manufacture of pharmaceutical composition The present invention discloses the use of laetispicine for manufacture of pharmaceutical composition for certain diseases caused by central nerves system monoamine neurotransmitter reuptake disorder. The isotope labeling central nerves system monoamine neurotransmitter reuptake test certifies the inhibiting activity of laetispicine to the reuptake of 5-HT, NE AND DA by rats’ synaptosomes. The present laetispicine can be used as raw material to prepare pharmaceutical composition which can inhibit the reuptake of central nerves system monoamine neurotransmitter, in order to treat the related diseases caused by reuptake of central nervessystem monoamine neurotransmitter.
US20090176817 Method of Treatment of Diarrhea-Predominant Irritable Bowel Syndrome in a Subject A method of improving stool frequency in a subject having diarrhea-predominant IBS, comprising administering a composition comprising cilansetron or a pharmaceutically acceptable derivative thereof to a subject in need of treatment in an amount sufficient to decrease stool frequency within 2 days or less of administering.
US20090092667 Method for Reducing Amyloid Deposition, Amyloid Neurotoxicity, and Microgliosis with (-)-Nilvadipine Enantiomer The present invention provides methods for reducing Aβ deposition, Aβ neurotoxicity and microgliosis in an animal or human afflicted with a cerebral amyloidogenic disease, such as Alzheimer's disease (AD), by administering therapeutically effective amounts of the (R)-enantiomer of the dihydropyridine compound nilvadipine, also known as (−)-nilvadipine, to the animal or human. Further provided are methods for reducing the risk of Aβ deposition, Aβ neurotoxicity and microgliosis in animals or humans suffering from traumatic brain injury by administering (−)-nilvadipine after the traumatic brain injury and continuing treatment for a prescribed period of time thereafter.
US20120035259 Controlled Release of Nitric Oxide And Drugs From Functionalized Macromers And Oligomers The present invention provides NO and, optionally, drug releasing macromers and oligomers wherein the drug molecule and NO releasing moiety are linked an absorbable macromer or oligomeric chain susceptible to hydrolytic degradation and wherein the macromer or oligomer comprises of repeat units derived from safe and biocompatible molecules such as glycolic acid, lactic acid, caprolactone and p-dioxanone. Furthermore, the present invention relates to controlled release of nitric oxide (NO) and/or drug molecule from a NO and drug releasing macromer or oligomer. Moreover, the present invention also relates to medical devices, medical device coatings and therapeutic formulations comprising of nitric oxide and drug releasing macromers and oligomers of the present invention.
CN102786458A Pyrrole formamide derivative, and preparation method and application thereof The present invention relates to compounds with a structure shown as a formula I or pharmaceutically acceptable salts thereof. R1, R2, R3, R4, R5 and R6 are defined as in the specification. The invention also provides a preparation method of the compounds with a structure shown as the formula I or pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the compounds and pharmaceutically acceptable salts thereof, and application of betulinic acid analogues or solvates thereof as active ingredients to preparation of antineoplastic medicaments for treating lung cancer, prostate cancer, colon cancer, leukemia, breast cancer, liver cancer, gastric cancer, pancreatic cancer, human malignant glioma and brain tumor.
US20100113393 Boronic Acid Salts Salts of a peptide boronic acid drug, for example of Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)2. The counter-ion to the boronate may be an alkali metal or derived from a strongly basic organic nitrogen-containing compound.
CA2791672A1 Positive allosteric modulators of mglur2 The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
CN101214299A Spray coating type empyrosis medicinal liquor and preparation thereof The present invention discloses a spraying burn and scald medicinal liquor, characterized in that the components includes 15 to 30 of burnet root, 100 of alcohol and 3 to 4 of sorghum straw. The alcohol concentration of the prepared medicinal liquor is 50 to 60 percent. The preparation method is that burnet root and sorghum straw are crushed and steam-cured for 10 to 20 days successively; then the raw materials are mixed with alcohol and stirred; the dense liquid is extracted, then packaged and stored. The present invention has the advantages of low cost and convenient preparation, and the good effects of detoxification, cooling and invigorating blood, alleviating pain, apocenosis, astringency, etc.
WO2014047782A1 Pharmaceutical composition containing resveratrol and resveratrol derivative and bcl-2 inhibitor and use thereof Provided in the present invention are a pharmaceutical composition containing resveratrol and resveratrol derivative and the use thereof in the preparation of medicine for treating colon cancer, liver cancer, lung cancer, kidney cancer, gastric cancer, brain tumours, sarcoma, glioma, pancreatic cancer, ovarian cancer, breast cancer or prostate cancer.
US7736622 Methods of diagnosing small intestinal bacterial overgrowth (SIBO) and SIBO-related conditions Disclosed is a method of treating small intestinal bacterial overgrowth (SIBO) or a SIBO-caused condition in a human subject. SIBO-caused conditions include irritable bowel syndrome, fibromyalgia, chronic pelvic pain syndrome, chronic fatigue syndrome, depression, impaired mentation, impaired memory, halitosis, tinnitus, sugar craving, autism, attention deficit/hyperactivity disorder, drug sensitivity, an autoimmune disease, and Crohn's disease. Also disclosed are a method of screening for the abnormally likely presence of SIBO in a human subject and a method of detecting SIBO in a human subject. A method of determining the relative severity of SIBO or a SIBO-caused condition in a human subject, in whom small intestinal bacterial overgrowth (SIBO) has been detected, is also disclosed.
WO2013018372A1 Amide derivative and drug containing same [Problem] To provide a novel amide derivative having greater safety and having superior phosphodiesterase 4 inhibition. [Solution] The novel amide derivative, which is represented by general formula (1), has strong PDE 4 inhibiting activity, and is rapidly metabolized in the body, thus having an activity that attenuates, and so it is possible to suppress systemic adverse effects from arising. From said characteristics, the compound of the present invention is particularly suited to localized administration. In formula (1), A represents a condensed aromatic heterocyclic group represented by formula (a) or formula (b).
CN1596908A Sterilization bacteria inhibition compound iodophor medicine and its preparation and preparation technology A compound tamed iodine for killing the bacteria on skin and mucosa by exterior applying is prepared from tamed iodine, and the composition of terbinafine hydrochloride and/or bunafine hydrochloride and/or fluconazole, etc.
US20100112091 Use of ramoplanin to treat diseases associated with the use of antibiotics The invention features a method of treating or preventing a disease associated with the use of antibiotics in a patient in need thereof by administering to the patient ramoplanin in an amount and for a duration effective to treat said disease. The disease may be caused, for example, by the presence of a bacterium such as enterotoxin producing strains of C. difficile, C. perfringens, or S. aureus.
US8394806 2-phenyl pyrazines as tubulin inhibitors Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
CN1559438A Medicine for treating tinea pedis, and prepn. method A medicine for treating fungal tinea pedis is prepared from salicyclic acid, benzoic acid, tannic acid and boric acid through grinding, proportional mixing, stirring and loading in color bag.
CA2809473A1 Stabilized ketorolac compositions Admixing carbon dioxide with an aqueous ketorolac solution is useful for increasing the stability of ketorolac in the carbon dioxide-admixed solution.
US20080234317 Methods for the improvement of memory and neurological function comprising the administration of compositions that act as inhibitors of the sodium proton (na+ /h+ ) exchanger, subtype 5 (nhe-5) The present invention comprises the use of pharmaceutical compositions that are effective in the inhibition of the Na+/H+ exchanger, subtype 5 (NHE-5) as inhibitors of cellular NHE-5 enhance long term potentiation (LTP) and are therefore effective in the treatment of memory impairments, dementing disorders, and for improving memory. Particularly suitable for the treatment of neurodegenerative disorders, memory impairments and dementing disorders, and for improving memory, are the following NHE-5 inhibitors of the formula I Wherein the R1-R8 substituents are further defined herein:
CN102379916A Bone mineral density increase capsule and preparation method thereof The present invention relates to a bone mineral density increase capsule and a preparation method thereof. The capsule comprises a capsule agent which is prepared from the following components: epimeddium, calcium carbonate, chitonsan and soybean extract. The preparation method comprises the following steps: crushing the epimeddium into coarse powder, performing ethanol backflow extraction; 2) merging extracting solution and filtering; 3) after mixing concrete with a formula amount of calcium carbonate, vacuum drying, crushing, and afterwards screening with a 80-100mesh sieve; 4) weighting chitosan, soybean extract and the obtained concrete powder, and mixing to uniform; and 5) filling the mixture into capsules and split charging. The bone mineral density increase capsule has an advantage of increasing the bone mineral density.
US20100297074 Wound healing compositions, systems, and methods The present disclosure relates, according to some embodiments, to the ability of SAP to suppress the differentiation of monocytes into fibrocytes. It also relates to the ability of IL-4 and IL-3 to enhance the differentiation of monocytes into fibrocytes. Methods and compositions for binding SAP, decreasing SAP levels and suppressing SAP activity are provided. Methods of using, inter alia, CPHPC, the 4,6-pyruvate acetyl of beta-D-galactopyranose, ethanolamines, high EEO agarose, IL-4, and IL-13, and anti-SAP antibodies and fragments thereof to increase monocyte differentiation into fibrocytes are provided. These methods are useful in a variety of applications, including wound healing. Wound dressings are also provided. Finally, the disclosure may include assays for detecting the ability of various agents to modulate monocyte differentiation into fibrocytes and to detect monocyte defects.
CN103393714A Local anesthesia pain-relieving time-delay agent A local anesthesia pain-relieving time-delay agent comprises: 0.5-20 mg of composite vitamin B, 10-20 mg of methylene blue, 10-100 mg of dexamethasone, 2-100 mL of a 5% sodium bicarbonate solution, and the balance 0.9% normal saline. The local anesthesia pain-relieving time-delay agent may also comprise 0.05-0.2 mg of hydrochloride adrenaline based on the need. The benefits comprise that: the local anesthesia pain-relieving time-delay agent is fast in effectiveness, only with 60 s; the local anesthesia pain-relieving time is long up to 30-40 days; no analgesic is needed after an operation, so that the risk of anaesthesia is reduced and security is improved; a patient subjected to the local anesthesia operation is conscious, and has no damaged central nerve and less-influenced whole body important function, and patient condition is easy to observe and control during operation; the patient is easy to nurse and transfer after the operation, manpower and material resources are saved, and the patient can easily recover physical ability after the operation; the amount of a local anesthesia medicine is reduced, and toxic and side effects are reduced; the local anesthesia pain-relieving time-delay agent is applied to subcutaneous or intramuscular injection in a local operation, the operation is simple and easy to grasp, so that the local anesthesia pain-relieving time-delay agent is applicable to vast grass-roots medical units; and the local anesthesia pain-relieving time-delay agent has a wide application scope comprising surgery, ophthalmology and otorhinolaryngology, gynaecology and obstetrics, plastics and aesthetic surgery and pain treatment department.
US20100178364 Dietary supplements against latent foreign DNA The invention presents methods for decreasing the concentration of a foreign polynucleotide in a human or animal subject, especially, when such polynucleotide is latent in the subject.
US20080287523 Pyrrolidin-3-Yl Compounds Useful as Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease The present invention is directed to pyrrolidin-3-yl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
US6861529 Cycloalkylpyrrole-3-carboxylic acid amide derivatives and heterocycloalkylpyrrole-3-carboxylic acid amide derivatives that bind with high affinity to the benzodiazepine site of GABA-A (gamma-aminobutyric acid) receptors This invention relates to cycloalkylpyrrole-3-carboxylic acid derivatives and heterocycloalkylpyrrole-3-carboxylic acid derivatives that bind with high selectively and/or high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in the treatment of central nervous system (CNS) diseases. This invention also relates to the use of these cycloalkylpyrrole-3-carboxylic acid derivatives and heterocycloalkylpyrrole-3-carboxylic acid derivatives in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the detection of GABAA receptors in tissue samples.
US7247734 In which the 3-phenyl group is 2,4-dihydroxy-substituted, e.g., 4-[5-bromo-4-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-6-chloro-benzene-1,3-diol; heat shock protein 90 inhibitors The present invention pertains to the use of certain 3,4-diarylpyazoles of formula (I), both in vitro and in vivo, to inhibit heat shock protein 90 (HSP90), and in the treatment of conditions mediated by HSP90, including, for example, cancer; wherein: Ar3 is independently: a C5-20aryl group, and is optionally substituted; Ar4 is independently: a C5-20aryl group, and is optionally substituted; R5 is independently: hydrogen; halo; hydroxyl; ether; formyl; acyl; carboxy; ester; acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamide; C1-7alkyl; C3-20heterocycyl; or C5-20aryl; RN is independently: —H; C1-7alkyl; C3-20heterocycyl; or, C5-20aryl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, such compounds for medical use, such compounds use in the treatment of conditions mediated by HSP90, including, for example, cancer, and use of such compounds in the preparation of medicaments for such treatments.
US20100004181 Combination comprising n-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-(1,3,4-oxadiazol-2-yl)phenyl) pyridine-3-sulphonamide and an lhrh analogue and/or a bisphosphonate A combination, comprising N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide, or a pharmaceutically acceptable salt thereof, and an LHRH analogue and/or a bisphosphonate is described.
CN103494895A Preparation method and application of bezoar antidote tablet The invention provides a preparation method of a bezoar antidote tablet. The bezoar antidote tablet is obtained by carrying out supercritical fluid extraction on the following raw herbal materials: 5g of bezoar, 50g of realgar, 200g of gypsum, 200g of rheum officinalem, 150g of scutellaria baicalensis, 100g of platycodon grandiflorum, 25g of borneol and 50g of liquorice, so that the content is greatly increased, and the dose is reduced. The invention also provides an application of the bezoar antidote tablet in preparation of a medicine for inhibiting the proliferation of a human nasopharyngeal carcinoma cell CNE-2Z.
WO2012012410A2 Kappa opioid receptor agonists The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, Rls R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
CN103554137A Preparation method of cefdinir micropowder The invention relates to a preparation method of cefdinir micropowder. The method comprises the following steps: adding cefdinir phosphate into cold water, adjusting the pH value to 6.8-7.1 by use of alkali liquor, adding active carbon, sodium hydrosulfite and EDTA (Ethylene Diamine Tetraacetic Acid), stirring, filtering and washing; mixing a filtrate and a washing liquid, and adding ethanol while stirring, wherein the addition of ethanol is 1/10 of weight of the cold water; adjusting the pH value to 4.1 by use of an acid, growing the grain for 15-25 minutes, continuously adjusting the pH value to 2.5-2.7 by use of an acid, stirring and growing the grain for 0.5-2 hours, cooling to 15-25 DEG C, stirring and growing the grain for 0.5-2 hours, cooling to 0-5 DEG C, and stirring and growing the grain for 0.5-2 hours; filtering and drying to obtain the cefdinir micropowder.
WO2008099165A1 Piperidine derivatives and their use for treatment of ccr8 mediated diseases The present invention provides compounds of formula (I) wherein n, R1, R2, R3 and R4 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
US20080241279 Materials and methods of using calcium for reduction of inflammation Nutritional approaches for the control of inflammation can involve the administration of therapeutic amounts of calcium. The administration of appropriate amounts of calcium to an individual results in a reduction in inflammatory processes and markers associated with the inflammatory processes. The therapeutic amount of calcium can be selected to change a level of inflammation in the individual. The approach for reducing inflammation can comprise a step of measuring the C-reactive protein marker level and administering calcium in amounts selected to induce a change in the C-reactive protein level. The calcium can be incorporated into a product with corresponding instructions to induce a desired inflammation reduction.
US20090258930 Double stranded rna structures and constructs, and methods for generating and using the same The present invention relates to novel double stranded RNA (dsRNA) structures and dsRNA expression constructs, methods for generating them, and methods of utilizing them for silencing genes. Desirably, these methods specifically inhibit the expression of one or more target genes in a cell or animal (e.g., a mammal such as a human) without inducing toxicity. These methods can be used to prevent or treat a disease or infection by silencing a gene associated with the disease or infection. The invention also provides methods for identifying nucleic acid sequences that modulate a detectable phenotype, such as the function of a cell, the expression of a gene, or the biological activity of a target polypeptide.
CN101292980A Pharmaceutical combination containing rapamycin for treating large intestine cancer The invention discloses a drug composite containing rapamycin for curing colorectal cancer. The drug composite is composed of PD98059 (2-amino-4-iso-oxygen flavone) and the rapamycin, the weight proportion of which is 292.4:1-1462:1. The invention can down regulate mTOR of colorectal cancer cells and the protein phosphorylation level of downstream p70s6K and 4E-BP1, so as to inhibit the proliferation activity of the colorectal cancer cells and simultaneously to block the growth cycle of the colorectal cancer cells, and then to inhibit the growth of human colorectal cancer cells and to reduce the incidence rate of the colorectal cancer and the tumor size in rats.
CN102485264A Pharmaceutical composition for treating children's long-term cough and preparation method thereof The invention discloses a pharmaceutical composition for treating a children's long-term cough and a preparation method thereof, and belongs to the field of modernization. The pharmaceutical composition for treating a children's long-term cough is prepared from 400 parts by weight of gypsum, 200 parts by weight of loguat leaf, 200 parts by weight of bamboo shavings, 200 parts by weight of mulberry leaf, 100 parts by weight of rhizoma pinellinae praeparata, 100 parts by weight of common coltsfoot flower, 100 parts by weight of white mulberry root-bark, 100 parts by weight of seed of pepperweed, 20 parts by weight of grassleaf sweelflag rhizome, 100 parts by weight of calcined bryozoatum, 50 parts by weight of wrinkled giant hyssop, 100 parts by weight of fried fructus perillae, 50 parts by weight of caulis lonicerae, 100 parts by weight of fried semen armeniacae amarae, 20 part by weight of agilawood, 100 parts by weight of fried muscardine silkworm and 6 parts by weight of herbal ephedrae. The pharmaceutical composition for treating a children's long-term cough has advantages that quality is stable and controllable; curative effects are obviously higher than curative effects of the same type of the existing pharmaceutical composition on the market; a taking dosage is reduced; bioavailability is improved; and economic and social benefits are remarkable.
CN101711757A High-efficiency sterilization disinfectant and preparation method thereof The invention relates to a sterilization disinfectant for efficiently killing fungi, which comprises pure water and mother liquor. The mother liquor is compound pure water-soluble mother liquor, and comprises the following components: 0.25 percent of chlorhexidine acetate, 0.01 percent of resin gel, 0.09 percent of sodium sulfacetamide, 0.15 percent of OP emulsifier and 95 percent of pure water. The sterilization disinfectant adopts a special dissolution dilution process, wherein the resin gel is viscous paste extracted from pure natural plants and can be a main dissolution catalysis substance after being diluted with physical pure water. By performing persistent heating, adding various effective components stage by stage and cooling the mixture, the chlorhexidine acetate can be completely dissolved into the pure water or distilled water; and the sterilization disinfectant is clear and transparent, can maintain the state of no turbidity and no precipitated flocs for at least two years, and has good stability. The sterilization disinfectant is characterized in that the sterilization disinfectant is highly sensitive to various fungi, and can be used for skin surface, mucous membranes or object surfaces.
DE102004002884A1 New aspernigrin B derivatives are intracellular calcium ion concentration reducing neuroprotective agents, useful for treating neurodegenerative diseases e.g. Parkinson's disease and multiple sclerosis Aspernigrin B derivatives (I) are new. - Aspernigrin B derivatives of formula (I) and their salts or solvates are new. - R1 - R7, X = H, optionally substituted 1-18C alkyl (including cycloalkyl), alkenyl, optionally substituted aryl (including heteroaryl), optionally substituted benzyl, acyl (e.g. CHO, COMe, COCCl3, fumaryl, maleyl, succinyl, COPh or branched, heteroatom-containing or aryl-substituted acyl), OH or SH (both optionally in tautomer form in the case of R1, R2 and R5 - R7), alkoxy (including cycloalkoxy, e.g. 1-4C alkoxy), alkylthio (e.g. SMe or SEt), substituted sulfonyl (e.g. SO3H, SO2Me, SO2CF3, SO2C6H4Me or SO2C6H4CH2Br), nitrogen substituent (e.g. NH2, NHR, NRR', NC or NO2), halo, CN or hetero-substituent; - R, R' = alkyl or aryl; - R8 = H, optionally substituted 1-18C alkyl (including cycloalkyl), alkenyl, optionally substituted aryl (including heteroaryl), optionally substituted benzyl, acyl (e.g. CHO, COMe, COCCl3, fumaryl, maleyl, succinyl, COPh or branched, heteroatom-containing or aryl-substituted acyl), alkoxy (including cycloalkoxy, e.g. 1-4C alkoxy), alkylthio (e.g. SMe or SEt) substituted sulfonyl (e.g. SO3H, SO2Me, SO2CF3, SO2C6H4Me or SO2C6H4CH2Br) or nitrogen substituent (e.g. NH2, NHR, NRR' or NRR'H2.Br); - Provided: - (1) Two or more substituent groups R1 - R8/X may be linked to form aromatic, heteroaromatic or at least partially saturated rings; and - (2) Aspernigrin B (Ia) is excluded as a new compound (I). - An INDEPENDENT CLAIM is also included for the use of aspernigrin B (Ia) as a compound of formula (I). - ACTIVITY - Neuroprotective; Cerebroprotective; Nootropic; Neuroleptic; Antiparkinsonian. - MECHANISM OF ACTION - Intracellular calcium ion concentration inhibitor. - Aspernigrin B (Ia) reduced the increase in intracellular calcium ion concentration in cultured neurones caused by the mGlu receptor agonist quisqualic acid. Pre-incubation of neurones with (Ia) at a concentration of 1 or 5 mu g/ml before incubation with quisqualic acid reduced the quisqualic acid-induced increase in the intracellular calcium ion concentration to 33.6% or 23.5% respectively of that in the absence of (Ia).
US20050187188 Methods for the treatment of a traumatic central nervous system injury The present invention provides methods for conferring a neuroprotective effect on a population of cells in a subject following a traumatic injury to the central nervous system. Specifically, the methods of the invention provide for the administration of a progestin or progestin metabolite following a traumatic brain injury. The progestin or progestin metabolite is administered at therapeutically effective concentrations that produce a neuroprotective effect (i.e., a decrease in the loss of neuronal activity) and reduces and/or prevents the various physiological events leading to neurodegeneration, such as, cerebral edema and the immune/inflammatory response.
WO2010052448A3 Fused pyrazine derivatives as kinase inhibitors A series of quinoxaline derivatives, and analogues thereof, which are functionalised further by a substituted phenyl or pyridinyl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
CN101690719A Bisulfate clopidogrel solid preparation, particles and preparation method thereof The invention relates to a bisulfate clopidogrel solid preparation, particles and a preparation method thereof. Particles contained by the solid preparation are solid mixture formed from bisulfate clopidogrel, cellulose excipients and molten adhesive with the melting point between 50 and 86 DEG, and an additionally added excipient of the particles contains weak alkaline lubricants and crosslinked polyvinylpyrrolidone. The solid preparation and the particles thereof are prepared by a melting-granulating method. The solid preparation has the advantages of solving sticking-picking problems existing in the preparation process, effectively reducing the degradation of clopidogrel during storage, reducing the incidence of transforming clopidogrel dextroisomer into clopidogrel levisomer and increasing the stability and security of the solid preparation.
WO2008109493A3 Nucleic acid compounds for inhibiting cd19 gene expression and uses thereof The present disclosure provides meroduplex ribonucleic acid molecules (mdRNA) capable of decreasing or silencing CD 19 gene expression. An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to a CD 19 mRNA. In addition, the meroduplex may have at least one uridine substituted with a 5-methyluridine, a nucleoside replaced with a locked nucleic acid, or optionally other modifications, and any combination thereof. Also provided are methods of decreasing expression of a CD 19 gene in a cell or in a subject to treat a CD19-related disease.
US20110053841 N-terminal fgf variants having increased receptor selectivity and uses thereof The present invention relates to the design, manufacture and use of fibroblast growth factor (FGF) polypeptides having improved receptor specificity. In particular, the invention relates to isolated FGF2 and FGF4 polypeptides that include a truncated N-terminus and optionally N-terminal amino acid substitutions. The present invention provides polypeptides, nucleic acids encoding the polypeptides, compositions of the same and methods for use thereof.
US7078186 Nucleotide sequences coding polypeptide for use in the prevention, diagnosis and treatment of tumor disorders The present invention relates to novel human apoptosis related polypeptides and isolated nucleic acids containing the coding regions of the genes encoding such polypeptides. Also provided are vectors, host cells, antibodies, and recombinant methods for producing human apoptosis related polypeptides. The invention further relates to diagnostic and therapeutic methods useful for diagnosing and treating disorders related to these novel human apoptosis related polypeptides.
CN101143129A Methotrexate intravenous emulsion and its preparation method The invention relates to a methotrexate combination, which is used for the vein transfusion and is in a stable oil-in-water emulsion. The invention also relates to the method of mixing the methotrexate into the oil to form the stable oil-in-water emulsion. The combination includes the methotrexate, the oil, the water and a surfactant.
EP2449114A1 Novel lipid formulations for delivery of therapeutic agents to solid tumors The present invention provides novel, serum-stable lipid particles comprising one or more active agents or therapeutic agents, methods of making the lipid particles, and methods of delivering and/or administering the lipid particles. More particularly, the present invention provides serum-stable nucleic acid-lipid particles (SNALP) comprising a nucleic acid (e.g., one or more interfering RNA molecules), methods of making the SNALP, and methods of delivering and/or administering the SNALP (e.g., for the treatment of cancer). In particular embodiments, the present invention provides tumor-directed lipid particles that preferentially target solid tumors. The tumor-directed formulations of the present invention are capable of preferentially delivering a payload such as a nucleic acid to cells of solid tumors compared to non-cancerous cells.
CN101376640A Low irritation garlicin derivative, and synthetic method and use thereof The invention discloses a garlicin derivative having the formula of (I), wherein a broken line optionally represents bond (double bond) or does not represent bond (single bond); n1 is an integer of 1 to 20; n2 is an integer of 2 to 4; R1, R2 and R3 are hydrogen or C1-20 alkyl; R4 is hydrogen or C1-20 alkyl; and when the broken line represents bond, n1 is 1, n2 is 3, and R4 is hydrogen, at least one of R1, R2 and R3 is C1-20 alkyl. Compared with garlicin, the garlicin derivative has the characteristics of enhanced antibacterial activity, and reduced irritation; and can be used for the preparation of an antibacterial drug; and also has garlic fragrance and taste, and can be used for the preparation of a spice or a flavoring agent. The invention also discloses a synthetic method of the garlic derivative, which comprises performing nucleophilic reaction of bromide having the formula (II) as initial raw material and sodium thiosulfate and sodium sulfide as nucleophilic reagent in solvent. The method is simple.
US20110152253 Spiroaminodihydrothiazine derivatives A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
CN103690505A Hypnotic double-layer controlled release tablet and preparation method thereof The invention provides a hypnotic double-layer controlled release tablet, comprising a rapid-release layer and a slow-release layer, wherein the rapid-release layer is provided with pores which are filled with rapid-release particles; the rapid-release layer and the rapid-release particles are composed of hypnotic drug and pharmaceutical excipients; the slow-release layer is composed of a hypnotic drug, a slow-release material and pharmaceutical excipients. The hypnotic double-layer controlled release tablet has the following technical effects that 1) the physical stability of the double-layer tablet provided by the invention is better than that of the common double-layer table, which is advantageous for storage and transportation, and 2) a dissolution test detects that the disintegration time limit of the rapid-release layer of the double-layer tablet provided by the invention ranges from 20 seconds to 30 seconds; and the slow-release layer is in a zero-order release pattern, and therefore the effectiveness and safety of medication for a patient are greatly improved. In the preparation process of the double-layer tablet, the rapid-release particles fill in the pores. The drug release pattern of combined rapid release and slow release guarantees that the rapid-release layer is disintegrated rapidly after the drug is taken; as a result, the blood concentration is capable of quickly reaching the therapeutic window range; the slow-release layer is slowly released so that the therapeutic action is maintained for a long period of time and toxic and side effects are effectively controlled.
US20070232656 Pharmaceutical Composition And Method For Treating Neurodegenerative Disorders The invention provides compositions and methods for treating neurodegenerative disorders. The method of the invention involves administering to an individual in need of treatment a composition having an acetylcholine esterase inhibitor and another therapeutic agent. The methods and compositions of the invention are useful for treating and preventing neurodegenerative disorders like Alzheimer's disease, dementia, and mild cognitive impairment.
CN103221412A (Aza)indolizine derivative and pharmaceutical use thereof Provided is a compound which is useful as a prophylactic or therapeutic agent for diseases or the like caused by abnormal serum urate level. An (aza)indolizine derivative represented by formula (I), said (aza)indolizine derivative having a xanthine oxidase inhibitory activity and being useful as a prophylactic or therapeutic agent for diseases caused by abnormal serum urate level, a prodrug thereof or a salt, etc. of the same. In formula (I), 0 to 2 of X<1> to X<4> represent a nitrogen atom and the remainder represent CR<1>; one of T<1> and T<2> represents cyano while the other represents a group represented by formula (A) [provided that when T<1> is cyano, at least one of X<1> to X<4> represents a nitrogen atom]; R<1>s independently represent a hydrogen atom, a halogen atom, a hydroxyl group, C1-6 alkyl, C1-6 alkoxy, etc.; the ring U represents a benzene ring, etc.; m is an integer of 0 to 2; and R<2>s independently represent a fluorine atom, a hydroxyl group, etc.
WO2014143630A1 Polymorph forms of desazadesferrithiocin analogs The present invention provides a solid form and compositions thereof, which are useful as metal chelators and which exhibit desirable characteristics for the same.
CN101284010B Application of di-(2,2'-dipyridine) copper complex with double-cation side arm in eliminating the superoxide ion free radical The invention discloses a technical proposal for eliminating ozone ion free radicals using di(2,2'-dipyridine)-copper complex with two cation side arms. The technical proposal comprises simulating hydrophobic environment of copper and zinc superoxide dismutase (Cu, Zn-SOD) active region and arginine residue with recognition function through ligating di(2,2'-dipyridine)-copper complex with quaternary ammonium ions having positive charges, so as to efficiently eliminate ozone ion free radicals. The technical proposal changes the thought of designing SOD substitute by simply simulating natural Cu, Zn-SOD active region structure in the prior art, and provides a new path of searching SOD analogues. Test results show that the SOD activity of the di(2,2'-dipyridine)-copper complex is better thanthat of all the analogues in the prior art, reaching half of the natural Cu, Zn-SOD from cattle erythrocyte and approaching the natural SOD from horseradish.
CN101584690A 2, 3, 3a, 4-tetrahydrothiochromeno2H-pyrazole serial compound with anticancer activity The invention discloses a sulfur-nitrogen contained ring heterocyclic compound, particularly a 2, 3, 3a, 4-tetrahydrothiochromeno2H-pyrazole compound with anticancer activities. Aiming at the current research and development situations of few anticancer medicines with large toxicity in the prior art, the 2, 3, 3a, 4-tetrahydrothiochromeno2H-pyrazole compound anticancer experiment is made, and an RPMI Medium 1640 is used as a cell culture medium and a detecting method which is an MTT method is adopted in the experiment. An experimental result indicates that the compound has high anticancer activities in vitro and can be used as the anticancer medicine.
EP2758403A2 Tricyclic compounds useful as neurogenic and neuroprotective agents The invention disclosed herein is direct to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in treating neurodegenerative diseases and promoting the generation or survival of neurons in the mammalian brain. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to a method of promoting the generation or survival of neurons in a patient in need thereof in neurodegenerative and related diseases.
EP0965340B1 Dermatologic preparation A dermatologic preparation which is reduced in side effects, has excellent percutaneous absorbability, and contains as the active ingredient an unsaturated fatty acid, which is a triglyceride represented by general formula (1), wherein one or two R1, R2, and R3 each represents a residue of a long-chain unsaturated fatty acid and the remainder represent(s) residue(s) of a medium-chain fatty acid. The triglyceride is preferably represented by formula (1) wherein one of R1, R2, and R3 represents a residue of a long-chain unsaturated fatty acid and the remainder represent(s) residue(s) of a medium-chain fatty acid. The long-chain unsaturated fatty acid is selected from the group consisting of eicosapentaenoic acid, docosahexaenoic acid, docosapentaneoic acid, arachidonic acid, alpha -linolenic acid, gamma -linolenic acid, linoleic acid, and dihomo- gamma -linolenic acid. The most desirable is the eicosapentaenoic acid residue or docosahexaenoic acid residue. The triglyceride is one obtained from a long-chain unsaturated fatty acid and/or a derivative thereof each having a purity of preferably 90 % or higher, more preferably 95 % or higher.
US20100047356 Charge-assembled capsules for phototherapy Novel phototherapeutic methods and compositions are described herein. Nanoparticle-assembled microcapsules as a new type of delivery vehicle for photosensitive compounds may be synthesized through a two-step assembly process. Charged polymer chains and counterions may be combined with a photosensitive compound to form photosensitive aggregates, and then nanoparticles may be combined with the aggregates to form the microcapsules. The shell may be composed of nanoparticles and/or polymer, and the core interior may contain the photosensitive compound. Formation occurs rapidly (on the order of seconds) and the conditions are very mild (at room temperature, in aqueous solution, and at neutral pH). The microcapsule synthesis is highly suitable as an encapsulation method, particularly for a charged photosensitive molecule like ICG.
US7414120 enhances ubiquitination of phosphorylated I kappa B; human E3 ubiquitin ligase polypeptides; inflammatory diseases, autoimmune diseases, cancer and viral infections Compositions and methods for modulating the activation of nuclear factor κB (NF-κB) are provided. The compositions comprise one or more agents that modulate ubiquitination of phosphorylated IκBα and/or IκBβ. Such compositions may be used for treating diseases associated with NF-κB activation. Modulating agents include human E3 ubiquitin ligases, antibodies thereto and variants thereof, as well as related proteins.
WO2013160354A1 Crystalline forms of saxagliptin Crystalline forms of saxagliptin It comprises a cocrystal of saxagliptin hydrochloride and a compound selected from the group consisting of saxagliptin, glycolic acid, malonic acid, and urea; or a solvate thereof, or a hydrate thereof. It also comprises a salt of saxagliptinwith glycolic acid 1:1 hydrate. It also comprises their preparation processes, as well as their use as antidiabetics.
US20080206365 2-hydroxy-2-substituted-3,10a-ethanophenanthrolines; inhibitors or activators for cytokine production; viricide, antiarthritic, anticarcinogenic, anticholesterol agents; myocardial infarction, osteoporosis, diabetes complications, sepsis, myeloma, transplant rejection, cirrhosis, AIDS, multiple sclerosis Provided are a certain compounds and compositions useful for inhibiting or activating the production of various types of cytokines. Also provided are certain compounds and compositions for preventing or treating various diseases attributable to abnormal cytokine production or compromised immunity.
US20050013875 Immunopotentiators in thermotherapy for cancer The present invention relates to an immunostimulator in hyperthermia of cancer, which contains a heat shock protein-inducing compound such as geranylgeranyl acetone, etc. The immunostimulator of the present invention can effectively regress tumor tissue that is difficultly treated by hyperthermia alone by combining with the hyperthermia, and also, metastasis of cancer can be effectively inhibited substantially without side effect.
WO2013190497A3 Compositions and methods for treatment of inflammatory diseases of the lung The invention provides pharmaceutical compositions and methods for treatment of an inflammatory disease of the lung caused by inhalation of a toxic agent or an irritant, more particularly, chlorine inhalational lung injury, as well as certain compounds of formulae (II) and (I) that are useful in such compositions and methods.
US7026358 Oral general anesthetics and metabolitically resistant anticonvulsants The present invention is directed to novel themisone derivative compounds that have been modified to prevent the formation of the toxic metabolite, 2-phenyl-acrylamide. Compositions comprising such derivative compounds have activity as anesthetics and as neuroprotective agents.
EP2044946A1 Preventive remedial therapeutic agent for phosphorus impairment, oral agent for adsorbing phosphate ion contained in food, beverage and chemical, and process for producing them The present invention provides agents for preventing, improving or treating phosphorus-related disorders and oral preparations; agents high in biosafety and phosphorus adsorptive power, which contain, as an active ingredient, ferric hydroxide as produced under such conditions that a ferrous species is present.
CN101015560A Compound suladime sulfadiazine sodium injection and its preparation The invention discloses an injection of compound m-sulfanilamide-methyl-pyrimidine sodium and its preparation method. the injection is prepared form m-sulfanilamide-methyl-pyrimidine sodium 50-20, naproxen 0.5-4, ofloxacin 1-8, and TMP 1-3 by dissolving m-sulfanilamide-methyl-pyrimidine sodium and ofloxacin in water in turn with opptionally booster solvent, stirring, dissolving TMP, naproxen in solvent respectively, merging the solutions, mixing uniformly, adjusting ph value, adding active carbon, stirring for adsorption for 15-20min, and adding water for injection to 1000 to obtain the final product. The injection can be used for treating general infection of livestock with rational formula and good therapeutic effect.
CN103483321A Alkyl linked pyridoin-quinolinone compounds and preparation method as well as application thereof The invention discloses alkyl linked pyridoin-quinolinone compounds. The compounds have a structural general formula which is shown in the specification. The compounds have better inhibition and killing effects on various pathogenic bacteria; a part of compounds have higher bacteriostatic activity than those of positive controls penicillin G, kalamycin and ketoconazole; the compounds can be used for preparing anti-infective medicaments. The invention discloses a preparation method of the compounds.
CN101411769A Medicament for treating beriberi and preparation method thereof The invention provides a medicine with good curative effect for treating beriberi and a method for preparing the same. The medicine comprises soaking medicine liquid and painting medical ointment, wherein the soaking medicine liquid is a medicine preparation prepared from the following materials in weight portion: kuhseng, cnidium fruit, dittany bark, scutellaria, yellow-corktree bark, astragalus, Chinese goldthread, isatis root, honeysuckle, bark of Chinese redbud, dandelion, pomegranate husk and root of pseudo-ginseng; and, the painting medical ointment is the medicine preparation which is prepared from the following materials in weight portion: cicada slough, wild chrysanthemum flower, spider and Kufan. The preparation method is as follows: the mixed material obtained by the mixing of the soaking medicine liquid is soaked in water, and boiled by soft fire, and the mixed material after boiling is filtered to be first medicine liquid and first medicine dregs; and, the first medicine dregs are soaked in water, and boiled by soft fire, and the first medicine dregs after boiling are filtered to be second medicine liquid and second medicine dregs; and, the preparation method of the painting medical ointment comprises the following steps: the wild chrysanthemum flower and the spider are added in the cicada slough, dried, mixed with the Kufan to be ground into powder to obtain the medical ointment powder, and the medical ointment powder is mixed with the vinegar to obtain the painting medical ointment.
US20130190407 Calcium receptor-active molecules The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.
CN102793700A Compound oil emulsion injection containing flumequine and preparation method thereof The invention discloses a compound oil emulsion injection containing flumequine and a preparation method thereof. The injection consists of the following raw materials in parts by weight: 10-25 parts of flumequine, 8-15 parts of naproxen, 4-5 parts of Twain-80, 35-60 parts of soybean oil for injection, 11-20 parts of poloxamer and 5-10 parts of water for injection. The preparation method comprises the following steps of: (1) dissolving the flumequine, naproxen and Twain-80 into the soybean oil for injection, sterilizing, and preserving heat to 60-75 DEG C for serving as an oil phase for later use; (2) dissolving the poloxamer into the water for injection, sterilizing, and preserving heat to 60-75 DEG C for serving as a water phase for later use; and (3) injecting the oil phase and the water phase into a homogenizer for mixing and emulsifying for 15 minutes, filtering, performing split charging, encapsulating and sterilizing to obtain the compound oil emulsion injection containing flumequine. In the method, the flumequine is compatible with the naproxen; and the prepared injection has the characteristics of high bioavailability, strong medicinal effect and the like, and can be used for resisting bacteria, diminishing inflammation, refrigerating and relieving pain.
CN1608623A Enteric coated donepezil hydrochloride tablet and its perpn process The present invention discloses enteric coated Donepezil hydrochloride tablet and its preparation process. The enteric coated Donepezil hydrochloride tablet is prepared with Donepezil hydrochloride as material medicine and proper amount of supplementary material. The enteric coated Donepezil hydrochloride tablet is used in treating light and medium degree senile dementia, and compared with gastric coated Donepezil hydrochloride tablet, the enteric coated Donepezil hydrochloride tablet has less side effects, no irritation to stomach and other advantages. Taking Donepezil regularly is beneficial to light and medium degree senile dementia patient.
CN1739511A Application of penehyliclidine hydrochloride in preparing medicine The present invention relates to the application of penehyclidine hydrochloride in preparing medicine, and is especially the application of penehyclidine hydrochloride in preparing medicine for resisting infectious shock. Animal experiment and clinical observation prove the curative effect of penehyclidine hydrochloride in resisting infectious shock and improving micro circulation. The present invention expands the medicinal use of penehyclidine hydrochloride.
EP1893583A1 Substituted aryloxy-n-bicyclomethyl acetamide compounds as vr1 antagonists This invention provides a compound of the formula (I): wherein A=B=D represents NR10-C(O)-NR9, S-C(O)-NR9, NR9-C(O)-S, NR9-C(O)-O, CR10-C(O)-NR9, 0-C(O)-NR9, NR10-C(O)-CR9, NR10-NR9-C(O), C(O)-NR9-NR10, NR10-N=CR9, N=N-CR9, NR10-CR9=N, N=CR9-NR10, NR10-N=N, N=N-NR10, S-CR9=N or N=CR9-S; X1 represents CR1 or N; X2 and X3 each independently represents CR8 or N; R1, R6, R8, R9 and R10 each independently represents hydrogen, halogen, hydroxy, (C1-C6)alkyl, (C1,-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)aikoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl or (C1-C6)alkylsulfonyl; R2, R3, R4, and R5 each independently represents hydrogen, (C1-C6)alkyl, halogen, halo(C1-C6) alkyl, or hydroxy(C1-C6)alkyl; and R7 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, [(C1-C6)alkyl]NH- or [(C1-C6)alkyl]2N-; or a pharmaceutically acceptable salt thereof, provided that: (i) when A=B=D represents NR10-N=N or N=N-NR10, then R2 represents (C1-C6)alkyl, halogen, halo(C1-C6) alkyl or hydroxy(C1-C6)alkyl; or (ii) when A=B=D represents NR10-N=N or N=N-NR10, and R2 represents (C1-C6)alkyl, then R7 represents halogen, (C1-C6)alkyl, (C1-C6)aIkOXy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkoxy, [(C1-C6)alkyl]NH- or [(C1-C6)alkyl]2N-. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
WO2006117548A1 Hydroxamic acid dervicatives as inhibitors of hdac enzymatic activity Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: formula (I) wherein Y1 is a bond, -(C=O)-, -S(O2)-, -C(=O)O-, -OC(=O)-, -(C=O)NR3, -NR3(C=O)-, -S(O2)NR3-, -NR3S(O2)-, or -NR3(C=O)NR5-, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, AIk1, AIk2 and Q are as defined in the claims; z is O or 1 ; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y); wherein R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, -(C=O)R3, -(C=O)OR3, or -(C=O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroary(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and B is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring B is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring.
WO2011017554A2 Val (8) glp-1 composition and method for treating functional dyspepsia and/or irritable bowel syndrome A method of treating functional dyspepsia and/or irritable bowel syndrome in mammals in need of treatment is disclosed herein. The method comprises administering to the mammal a formulation by inhalation, wherein the formulation avoids first pass metabolism of the active ingredient. The method comprises administering a formulation by pulmonary inhalation comprising a diketopiperazine and a glucagon-like peptide (GLP-1 ), analog, ROSE-010.
EP1517682B1 Pharmaceutical formulation comprising non-peptide renin inhibitor and surfactant Composition comprising (1) a non-peptide renin inhibitor which is poorly soluble to readily soluble in water and (2) at least one physiologically tolerated anionic surfactant, at least one physiologically tolerated amphoteric surfactant, at least one physiologically tolerated neutral surfactant, or a mixture of at least two of these surfactants, with the quantity of readily soluble renin inhibitor being at least 10% by weight, and the quantity of a poorly soluble renin inhibitor being at least 35% by weight, based on the composition. In oral administration forms, the composition exhibits increased bioavailability.
CN101780034B Cefathiamidine suspension and novel application thereof The invention discloses cefathiamidine suspension, which comprises cafathiamidine, a carrier, an emulsifier, an emulsion assistant and a freeze-drying additive, wherein the ratio of the cefathiamidine, the carrier and the emulsifier by weight is 1: 0.5 to 2: 0.5 to 1. The invention also discloses a preparation method of the cefathiamidine suspension and an application thereof for preparing drugs for treating secretory otitis media. The cefathiamidine suspension has the advantages of high stability, long retention period, good targeting property, good quick solubility and the like.
US20100227838 Combination Therapy for Treating Cancer and Diagnostic Assays for Use Therein The present disclosure relates to a combination of therapeutic agents for use in treating a patient a subject suffering from cancer. In addition, the present disclosure also relates to diagnostic assays useful in classification of patients for treatment with one or more therapeutic agents.
EP2561871A1 Diarylhydantoin compounds as androgen receptor antagonists for treatment of cancer The present invention relates to diarylhydantoin compounds of the formula below, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer by acting as androgen receptor antagonists (AR antagonists).
CN101062066A Compound isatis-root injection for animals and the preparing method thereof The invention discloses a compound isatic root injection for animals and preparation technology, which is characterized by the following: allocating main medicine, adjunct and dissolvent; choosing the main medicine from isatic root, linbevelin, moroxydine and amantadine hydrochloride; choosing the adjunct from anti-oxidant, metal chelating agent and dissolvent for injection. This invention possesses advanced productive technology and long shelf life.
DE102004054053A1 New 2-(hetero)aryl-imidazoline or tetrahydropyrimidine derivatives, are bradykinin B1 receptor antagonists used e.g. for treating neuropathic or inflammatory pain or migraine (Hetero)arylsulfonyl-substituted 2-(hetero)aryl-2-imidazoline or -1,4,5,6-tetrahydropyrimidine derivatives (I) are new. Imidazoline or tetrahydropyrimidine derivatives of formula (I), and their tautomers, enantiomers and diastereomers (including mixtures) and salts, are new. R1>phenyl or heteroaryl; R4>H or 1-6C alkyl; m : 2 or 3; Ar : phenylene or heteroarylene; A : -CO-NR3>-(CH2)n-NR2>-, -NR3>-CO-Q1>-NR2>-, -Q2>-CH2CH2-NR2>-, -NR3>-CO-CH2CH2-Q3>-, -NR3>-CO-(CH2)o-NR2>-, -CO-Q4>-, -NR3>-CO-CH2-Q3>- or -NR3>-CO-Q5>-; Q1>cyclopentane-1,3-diyl or cyclohexane-1,3-diyl; Q2>2-oxo-imidazolidine-1,3-diyl or 2-oxo-hexahydropyrimidine-1,3-di yl; or 2-oxo-pyrrolidine-1,3-diyl or 2-oxo-piperidine-1,3-diyl (both attached to CH2CH2-NR2> in the 3-position); Q3>pyrrolidine-1,2-diyl or piperidine-1,2-diyl (both attached to NR3>-CO-CH2CH2 or NR3>-CO-CH2 in the 2-position); Q4>piperazine-1,4-diyl or homopiperazine-1,4-diyl; Q5>pyrrolidine-1,3-diyl or piperidine-1,3-diyl (both attached to NR3>-CO in the 3-position); n : 2 or 3; o : 1-3; R2>H, 1-6C alkyl, 2-3C alkenyl, 2-3C alkynyl, 3-7C cycloalkyl or Ph; R3>H, 1-6C alkyl, 2-3C alkenyl, 2-3C alkynyl or 3-7C cycloalkyl; heteroaryl moieties : 5- or 6-membered monocyclic heteroaryl, where 6-membered heteroaryl contains 1-3 N as heteroatom(s) and 5-membered heteroaryl contains (i) one N(Q6>), O or S, (ii) one N(Q7>), O or S plus one N or (iii) one N(Q8>) plus 2 or 3 N as heteroatom(s); Q6>H, 1-3C alkyl, Ph or phenyl-(1-3C) alkyl; Q7>H, 1-3C alkyl, Ph, amino-(2-3C) alkyl, (1-3C) alkylamino-(2-3C) alkyl, di-(1-3C) alkylamino-(2-3C) alkyl, 4-7 membered cycloalkyleneimino-(1-3C) alkyl or phenyl-(1-3C) alkyl; Q8>H, 1-3C alkyl or phenyl-(1-3C) alkyl; the methyl or ethyl groups are optionally substituted by one or more F; and phenyl groups are optionally substituted by 1-3 of halo, 1-3C alkyl, CF3, 1-3C alkoxy or OCF3. [Image] - ACTIVITY : Analgesic; Antimigraine; Antiinflammatory. - MECHANISM OF ACTION : Bradykinin B1 receptor antagonist. The hydrochloride of 3-(1-(4-chloro-2,5-dimethyl-benzenesulfonyl)-pip eridin-2-yl)-N-(2-(4-(4,5-dihydro-1H-imidazol-2-yl)-phenyl)-ethyl)-N- methylpropionamide (Ia) had Ki 26 nM in an hBK1 receptor binding assay.
US20100190856 Novel Polyhydroxylated Compounds as Fatty Acid Synthase (FASN) Inhibitors The present invention relates to new polyhydroxylated compounds and, in particular, to its activity as fatty acid synthase (FASN) inhibitors and to their use for the treatment of pathological states for which an inhibitor of this enzyme is indicated. The invention further relate to pharmaceutical compositions containing them and to a process for the preparation of such compounds.
EP2219616A2 Lyophilized pharmaceutical composition with improved stability containing taxane derivatives, and method of manufacturing the same The present invention relates to a lyophilized pharmaceutical composition for injection having superior storage stability comprising a taxoid, and a method thereof. More specifically, the present invention relates to a lyophilized pharmaceutical composition for injection having improved solubility and stability of dilution compared to the conventional preparations by dissolving a water-insoluble taxoid in distilled water added with a hydrophilic polymer such as hydroxypropylmethyl cellulose(HPMC), polyethylene glycol (PEG) or polyvinylpyrrolidone(PVP)cyclodextrin (CD), and lyophilizing the mixture and a method thereof.
WO2013071217A1 Dihydropteridinones Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.
CN101224220A Compounds for strengthening organism immunity function and application thereof The invention provides a combination used for enhancing organism immune function. The active components of the invention are astragalus polysaccharide and 20(S)-protopanaxadiol. The combination use of the astragalus polysaccharide and 20(S)-protopanaxadiol can enhance the organism immune function. Pharmacological tests show that the combination use of the two components is superior to separation use of each of the two components on the function of enhancing thymus index of normal mice, the CTX of which is decreased. 20(S)-protopanaxadiol can promote the immune regulation effect of the astragalus polysaccharide.
US20100209418 Solid Forms of a Raf Kinase Inhibitor The present invention is directed to solid forms of the Raf kinase inhibitor 1-methyl-5-(2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazol-2-amine, as well as compositions thereof and uses of the same.
CN102617465A Tacrine-caffeic acid hetero-blends, their preparation method and medicinal compositions The invention relates to synthesis of a series of tacrine-caffeic acid hetero-blends and derivatives, a preparation method thereof, medicinal compositions containing them, and their medical application. The structural formula of the tacrine-caffeic acid hetero-blends is shown as formula (I). By changing substituent groups and joints, the inhibitory activity to AChE (acetylcholinesterase) and selectivity to AChE/BuChE (butyrocholinesterase), as well as antioxidant activity can be adjusted. And AChE-induced Abeta (amyloid-beta peptide) aggregation can be inhibited. The tacrine-caffeic acid hetero-blends and derivatives can be prepared into appropriate medicinal dosage forms to treat Alzheimer's disease and other related dementia. The invention belongs to the medical field.
US20120289505 Inhibitors of diacylglycerol acyl transferase The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
WO2012062653A1 Combination of bevacizumab and 2,2-dimethyl-n-((s)-6-oxo-6,7-dihydro - 5h-dibenzo[b,d]azepin-7-yl)-n'-(2,2,3,3,3-pentafluoro-propyl)-malonamide for the treatment of proliferative disorders The present invention relates to a combination therapy of 2,2-dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N'-(2,2,3,3,3-pentafluoro-propyl)-malonamide, or a pharmaceutically-acceptable salt thereof, and bevacizumab for treating a patient suffering from a proliferative disorder, in particular a solid tumor, for example a brain tumor.
US20090275590 (1-azinone)-substituted pyridoindoles Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5; is H, optionally substituted alkyl, optionally substituted heterocycle, —C(═O)—R6, —C(═O)—O—R7, or —C(═O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH═CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.
US20050054584 Reducing weight and damage cuased by diabetes; antidiabetic agents The invention relates to the use of a substance being selected from the group consisting of “sugar phosphates, sugar phosphate analogs, amino acids, amino acid analogs, and mixtures of said substances” for producing a pharmaceutical composition for reducing weight and/or preventing delayed damage caused by diabetes mellitus by modulating the association p36/malate dehydrogenase and/or transaminases.
CN102167720B Betulonic acid derivant for restraining differentiation of osteoclast, preparation method thereof and application thereof The invention relates to a betulonic acid derivant for restraining the differentiation of osteoclast, a preparation method thereof and application thereof. The preparation method comprises the steps of adding betulonic acid and di-brominated mair multi-yeast acid into absolute ether, stirring for 4h at a room temperature, and purifying; and adding thioacetamide and absolute ethyl alcohol, reacting in a reflowing way for 12h, concentrating and extracting reaction liquor, merging an organic layer, washing by saturated saline water, evaporating off an organic solvent, and purifying a coarse product by means of silicagel column chromatography to obtain the betulonic acid derivant I. By improving the structure of natural product betulonic acid and introducing a benzo heterocyclic ring into a C2 site and a C3 site, the method is used for effectively synthesizing the novel betulonic acid derivan, and the synthesis method is simple and convenient; and by improving the structure of the betulonic acid, the function of the compounds for restraining the differentiation activity of the osteoclast is obviously improved.
WO2012025054A1 Diimidated derivative of berbamine, and preparation method therefor and use thereof The present invention relates to a novel diimidated derivative of berbamine of General Formula I, comprising, but not limited to, a phthalimidated derivative of berbamine, an aromatic heterocyclic dicarboximidated derivative of berbamine, or a pharmaceutically acceptable salt thereof, a method for preparing the compounds, a pharmaceutical composition comprising the compounds, and a use of the compounds in preparation of anti-tumor drugs.
CN102503999A Demalonyl azalomycin F derivatives, preparation method thereof and use in preparing microbicides The invention discloses demalonyl azalomycin F derivatives, a preparation method of the demalonyl azalomycin F derivatives and use in preparing microbicides. The method comprises the following steps of: allowing azalomycin F to react with alcohols in an acidic alcoholic solution to produce azalomycin F derivatives, and hydrolyzing in an alkaline methanol aqueous solution to remove malonyl groups, to obtain demalonyl azalomycin F derivatives. The antimicrobial test shows that the MIC (minimal inhibitory concentration) of demalonyl azalomycin F derivatives against the test strains is 0.39 to 1.56 Mug/mL and the activity is 4 to 8 times the activity of azalomycin F. The cytotoxicity test shows that the cytotoxicity of demalonyl azalomycin F derivatives to the cell line HCT-116 is significantly less than that of azalomycin F. The demalonyl azalomycin F derivatives are proved to have a significant antimicrobial effect and a low toxicity, can be used for preparing microbicides, and has good development prospects.
CN101305997A Medicament for treating nerve dysfunction after refraining opium type material The invention relates to a drug for treating the nerve functional disturbance after the withdrawal of opium matters. The drug is a compound preparation which is composed of atropine and baclofen in the mass ratio of 1:1-10. The drug has the main function that the nerve functional disturbance syndrome which is caused by the withdrawal after opioid addiction can be inhibited. The compound preparation can well inhibit the withdrawal syndrome, which is beneficial for the physical recovery. The detoxification drug with the advantages of low use cost, safety, reliability, strong scientificity, and insignificant toxicity and side effects can shorten the withdrawal time relieve or partially remove the nerve functional disturbance syndrome after the withdrawal of the narcotics, and can be used as an ideal detoxification drug.
CN102731401A Geldanamycin derivatives, preparation method thereof, and uses thereof The invention relates to new geldanamycin derivatives, a preparation method of the compounds, and uses of the compounds in the preparation of cell killing agents for killing activities of cells, cell proliferation inhibitors and antitumor medicines. The invention also relates to a medicinal composition containing the compounds. The compounds of the invention can be used for treating diseases of excess cell propagation, such as cancers and the like.
EP1635856A2 Saposin c-dops: a novel anti-tumor agent Compositions and methods for treating subjects with disorders characterized by hyper-proliferating cells such as tumors and cancers are provided. The compositions comprise agents that are combinations of saposin C ( or prosaposin-related polypeptides and dioleoylphosphatidylserine ( or inner leaflet components ). This anti-tumor agent is administered in the methods of the invention according to a dosing regimen. Administering an agent of the invention results in a positive therapeutic response in a subject with a tumor.
WO2008099414A1 NOVEL CATIONIC 17 α- SUBSTITUTED-ESTRADIOL DERIVATIVES USEFUL AS ANTI-CANCER AGENT The present invention provides a novel series of cationic, lipid-based, 17α-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17α-substituted-estradiol derivatives. The invention also provides information about highly selective anticancer activities of these molecules in estrogen responsive cell lines. The compound elicits high level of toxicity to gynecological cancer cell lines such as MCF-7, T47D (estrogen receptor positive cell lines), MDA-MB-468 (estrogen receptor knock-out cell line), HeIa (cervical cancer). The present class of cationic lipid-based, estradiol derivatives is likely to find specific use in developing target specifically deliverable anticancer drugs for the treatment of gynecological cancers that are most prevalent in women population irrespective of ethnicity.
EP1204426B1 Medical preparation for treating arthrosis, arthritis and other rheumatic joint diseases The invention relates to a medical preparation for treating arthrosis, arthritis and rheumatic joint diseases comprising a suspension consisting of one-shelled or multi-shelled nanoscalar particles composed of a core containing iron oxide and of an inner shell with groups that are capable of forming cationic groups or, optionally, of at least one outer shell with neutral and/or anionic groups. Radionuclides and substances, said substances being cytotoxically active when subjected to the influence of heat, are bound to the inner shell. The preparation which is injected into the joint cavity and which is subjected to a magnetic alternating field promises an excellent treatment outcome due to the high rate of phagocytosis and the trimodal combinatorial effect of thermotherapy, radiotherapy and chemotherapy.
CA2195759C Tetrahydropyridinylmethyl derivatives of pyrrolo[2,3-b]pyridine A class of pyrrolo[2,3-b]pyridine derivatives of formula (I), wherein Q represents a moiety of formula Qa or Qb, are ligands for dopamine receptor subtypes within the body, in particular the dopamine D4 receptor subtype and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia.
CN101249082A Preparation of acidum citricum tamoxifen polylactic acid-glycolic co-polymer microballoons The invention relates to a preparation method of tamoxifen citrate polylactic acid-glycolic acid copolymer microspheres. The method comprises the following steps: 1) dissolving polylactic acid-glycolic acid copolymer (PLGA) in an organic solvent, adding tamoxifen citrate, and dissolving under ultrasonic action to obtain a solution as organic phase; 2) adding slowly the organic phase into aqueous solution of polyvinyl alcohol (PVA) as water phase under stirring, adding electrolytes, stirring at room temperature until the organic solvent volatilizes completely, centrifugating, washing, and freeze-drying to obtain tamoxifen citrate polylactic acid-glycolic acid copolymer microspheres. The microsphere has round shape, uniform particle size distribution (below 10 micrometers), high drug content (above 10%), high encapsulation rate (about 80%), and in vitro release characteristics of long-acting preparations; and is suitable for the use as implant for prevention and treatment of breast cancer.
US7153946 Molecular conjugates for use in treatment of cancer A molecular conjugate is provided having the formula: wherein R1 is a de-hydroxyl or de-amino moiety respectively of a hydroxyl-bearing or amino-bearing biologically active molecule or an analog or derivative thereof, and Z is —O— or —NH—, respectively, Y is a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups; and R2 is —CH═CH(W), —CH(OH)CH(OH)W, or —C(O)H, where W can be H, a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups.
EP1066286B1 Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors Novel heterocyclo-substituted imidazopyrazines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.
WO2013146754A1 Aromatic heterocyclic five-membered ring derivative having trpv4 inhibitory activity The present invention relates to: a compound represented by formula (I) or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition which contains the compound or the salt. (In formula (I), R1 represents a hydrogen atom, a substituted or unsubstituted alkyl, a substituted or unsubstituted aromatic carbon ring group or the like; X represents -N(R3)-, -O- or -S-; Y represents =C(R4)- or =N-; Z represents -N(R7)-, -O- or -S-; R2 represents a substituted or unsubstituted alkyloxy or a group represented by formula -(CR2aR2b)n-R2c (wherein each R2a independently represents a hydrogen atom, a halogen or the like; each R2b independently represents a hydrogen atom, a halogen or the like; R2a and R2b bonded to the same carbon atom may combine together to form an oxo, a substituted or unsubstituted non-aromatic carbon ring or the like, and two R2a moieties bonded to adjacent carbon atoms and/or two R2b moieties bonded to adjacent carbon atoms may combine together to form a single bond; R2c represents a substituted or unsubstituted aromatic carbon ring group or the like; and n represents an integer of 1-3); each of R3 and R7 independently represents a hydrogen tom, a substituted or unsubstituted alkyl or the like; each of R4 and R5 independently represents a hydrogen atom, a halogen, a substituted or unsubstituted alkyl or the like; and R6 represents a hydrogen atom, a halogen, a substituted or unsubstituted alkyl or the like.)
CN1887871A 2,6-diamino-3,5-dinitrile-4-aryl pyridine derivative and its synthesis and application The present invention relates to one kind of medicine compound, and is especially 2, 6-diamino-3, 5-dinitrile-4-aryl pyridine derivative and its synthesis and application. The 2, 6-diamino-3, 5-dinitrile-4-aryl pyridine derivative in the structure as shown is synthesized with aromatic amine, aromatic aldehyde and malononitrile as materials, ethanol as solvent and piperidine or Lewis acid as catalyst. The synthesis process has simple operation, easy separation, high yield and environment friendship, and is favorable to industrial production. The synthesized 2, 6-diamino-3, 5-dinitrile-4-aryl pyridine derivative possesses activity of resisting Helicabacter pylori, and may be used in preparing medicine for resisting Helicabacter pylori.
WO2011103126A1 Treatment of metabolic syndrome with piperidine amides The present invention relates to piperidine derivatives of formula (I) and (II), their pharmaceutical compositions and methods of treatment of metabolic syndrome disorders such as obesity, diabetes, hypertension and hyperlipidemia using the said compounds. Formula (I) Formula (II) In formula (I), X and Y represent optionally substituted aryl or heteroaryl; R1 represents H or optionally substituted lower alkyl; R2 represents H, optionally substituted lower alkyl, ester, optionally substituted alkoxycarbonyl, acyl, thioester, thioacyl, thioether, optionally substituted alkoxyl, amino, optionally substituted aminoalkyl, amido or acylamino; and R3 represents H or OH. In formula (II), X represents optionally substituted aryl or heteroaryl; R4 represents H or optionally substituted lower alkyl; and R5 represents optionally substituted lower alkyl.
CN103610687A Application of engeletin in preparing medicines for treating or preventing chronic renal injury The invention relates to an application of engeletin in preparing medicines for treating or preventing chronic renal injury, and specifically relates to an application of engeletin in preparing medicines for treating or preventing chronic renal failure, renal fibrosis and diabetic nephropathy. In the application, the dosage range of engeletin is 10-500mg, preferably 10-250mg. The engeletin exists in forms of troches, pills, granules, capsules, syrups and the like, preferably capsules.
US20090298785 Method for Treating Ocular Cancer It has now been found that the p53 pathway is inactivated in ocular cancers such as retinoblastoma. As such, the present invention is a method for inducing ocular cancer cell death using a p53 activator. In particular embodiments, the p53 activator blocks the interaction between DM2 or DMX and p53. As the p53 activator induces ocular cancer cell death, a method for preventing or treating ocular cancer is also provided.
CN102532262A Preparation of fatty acid-RGD-fatty alcohol conjugate mediated epirubicin targeted liposome and evaluation on anticancer activity The invention discloses preparation of fatty acid-RGD-fatty alcohol conjugate mediated epirubicin targeted liposome and evaluation on anticancer activity. According to the invention, the conjugate has the following structural formula: CH3(CH2)nCO-Arg-Gly-Asp-OCH2(CH2)10CH3, wherein n is equal to 4-16. An anticancer medicine is introduced into the conjugate to obtain anticancer targeted liposome medicine; the liposome can increase the concentration of the anticancer medicine at a target position, reduce the toxic and side effects of the anticancer medicine at a non-target position, and improve the therapeutic index of the medicine.
US20120328683 Alkylaminoalkyl oligomers as broad-spectrum antimicrobial agent The present application relates to oligomeric antimicrobial compounds and compositions comprising the same. The oligomers are formed by polymerizing aminoalkyl (meth)acrylate or aminoalkyl (meth)acrylamide monomer(s). In addition to imparting materials with broad spectrum antimicrobial activity, the oligomers can impart antimicrobial activity to substrates such as hair and skin.
US20080027019 Oligonucleotide compositions and methods for the modulation of the expression of b7 protein Compositions and methods for the treatment of asthma with oligonucleotides which specifically hybridize with nucleic acids encoding B7 proteins.
WO2012173682A3 Compounds and methods for the treatment of isocitrate dehydrognase related diseases The invention relates to compounds of Formula I pharmaceutically acceptable salt, ester or prodrug thereof:
CN102397452A Submicron powder cough powder normal temperature preparation method and special two-way airflow screen grader The invention discloses a submicron powder cough powder normal temperature preparation method, which comprises the following steps that: rhizoma anemarrhenae, bitter orange, herba ephedra, balloon flower, bitter almond, lepidium seeds, cortex mori radicis, dried orange peel, gypsum, peucedanum root, blackberry lily, folium eriobotryae and liquorice are weighed according to proportion, dried and pulverized, and oil in the bitter almond and the lepidium seeds is extracted; the coarse powder and the dregs of the bitter almond and the lepdium seeds are mixed and are placed inside a rod mill to bepulverized, then the mixed powder is blown into a special two-way airflow screen grader to be screened to obtain the powder with the granularity being less than or equal to 25nm, and the powder is conveyed by the airflow produced by a draught fan into a cyclone collector to be collected and to obtain the cough submicron powder; the powder cannot pass through a 500-mesh sieve is collected by a funnel and is conveyed into the rod mill through a pipeline to be circularly pulverized; and the cough submicron powder finished product is obtained by adequately mixing the cough submicron powder and the bitter almond oil and the lepdium seed oil. The preparation method has the advantages that: the entire preparation process is carried out under the normal temperature, and the granularity of the finished product medicine is less than or equal to 25nm; and the two-way airflow screen grader which is utilized in the method can simplify the preparation process of the submicron powder cough powder.
WO2014154131A1 Caffeoyl substituted pentacyclic triterpene derivative and use thereof Provided are a caffeoyl substituted pentacyclic triterpene derivative as represented by formula (I) and pharmaceutical composition containing the same. Also provided are uses of the derivative in the preparation of drugs or health-care products for preventing and treating brain injury induced by cerebral ischemia, glucose deprivation, and cerebral anoxia, and/or nervous dysfunction, and/or cognitive dysfunction.
WO2012073025A1 Glucosaminoglucans such as heparin for use in the treatment of pulmonary inflammation such as copd According to the invention there is provided heparin for use in the treatment of COPD, wherein, after administration to a subject, the heparin reduces inflammation in the lungs of the subject.
CN101812105A Cytarabine 5'-O-amino-acid ester, salts thereof and preparation method thereof The invention belongs to the technical field of medicines and discloses cytarabine 5'-O-amino-acid ester, pharmaceutically acceptable salts thereof and a preparation method thereof. The preparation method comprises the following steps of: slowly dropping carbobenzoxy chloride into a solution formed by cytarabine, sodium bicarbonate and N,N-dimethylacetylamide, and obtaining a compound A after reacting at room temperature; using the compound A and N-butyloxy formoxyl-amino acid as raw materials; adding a reagent to the solution to carry out an esterification reaction to obtain the cytarabine 5'-O-amino-acid ester; and then adding acid to obtain a finished product. The pharmaceutically acceptable salts comprise hydrochlorides, sulfates, formates, acetates, mesylates, propionates, butyrates, p-toluene sulphonates, phosphates, bisulfates, maleates, lactates, carbonates, bicarbonates, malonates, and salts formed with acidic amino acids, and the like. The invention can obviously improve the membrane permeability of the cytarabine so as to improve the bioavailability of the cytarabine.
US20130018092 Treatment for hypoxia The invention provides a method for treating hypoxia in a normal subject, comprising administering 5-HMF to the subject.
WO2010147434A2 Use of toosendanin or melia azedarach extracts for preventing or treating dementia The present invention relates to a composition for preventing or treating dementia containing toosendanin or Melia azedarach extracts as active ingredients, and more specifically, to a pharmaceutical composition for preventing or treating dementia containing toosendanin or Melia azedarach extracts as active ingredients. The pharmaceutical composition containing Melia azedarach extracts, toosendanin or pharmaceutically acceptable salts thereof as active ingredients, use thereof, and a method for preventing and treating dementia are effective in preventing or treating dementia. Especially, the composition, use, or method of the present invention are especially excellent in promoting APPa generation which suppresses beta-amyloid generation and protects nerve cells, and thus has high efficiency in preventing or treating dementia such as Alzheimer's disease.
US7846451 Chimeric outermembrane polypeptide for use as tool in diagnosis and treatment of parasitic infection The invention discloses the Moraxella catarrhalis outer membrane protein polypeptide and polypeptides derived therefrom (collectively “OMP21”), nucleotide sequences encoding said OMP21, and antibodies that specifically bind OMP21. Also disclosed are pharmaceutical compositions including prophylactic or therapeutic compositions, which may be immunogenic compositions including vaccines, comprising OMP21, antibodies thereto or nucleotides encoding same. The invention additionally discloses methods of inducing an immune response to M. catarrhalis and OMP21 in an animal, preferably a human, methods of treating and methods of diagnosing Moraxella infections in an animal, preferably a human, and kits therefor.
WO2006077425A1 Combinations of pyrazole kinase inhibitors and further antitumor agents The invention provides a combination of a compound having the formula (0) and two or more further anti-cancer agents: or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C=O, NR9(C=O) or 0(C=O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1 , 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).
WO2010040012A1 Compositions and methods for reducing triglyceride levels The present invention is directed to methods of reducing plasma triglyceride level in subjects by administering docosahexaenoic acid (DHA). The method can comprise administering daily to the subject a dosage form comprising docosahexaenoic acid ester substantially free of eicosapentaenoic acid (EPA), wherein the DHA is derived from an algal source. In some embodiments, the method comprises administering daily to the subject a dosage form comprising DHA ester substantially free of EPA, wherein the DHA ester is about 60 % to about 99.5 % (w/w) of the total fatty acid content of the dosage form. In some embodiments, the method comprises administering daily to the subject a dosage form comprising about 200 mg to about 4 g of DHA ester substantially free of EPA. In some embodiments, the foregoing methods also result in a lowering of the amount of total cholesterol in the subject.
EP2386545A1 Heteroaryl ureas containing nitrogen hetero-atoms as P38 kinase inhibitors This invention relates to the use of a group of heteroaryl ureas containing nitrogen in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.
WO2012146057A1 Curcuminoid injection solution and intravenous injection Disclosed is a curcuminoid injection solution mainly composed of curcuminoid, a solvent used for injection and a small amount of pH adjusting agent. Also provided is a curcuminoid intravenous injection which simply mixes the aforementioned injection solution with an emulsion at a volume ratio of 1:5 to 1:250. After mixing the curcuminoid injection solution and the emulsion, the drug loading of the curcuminoid in the intravenous injection can attain 1.5 mg/ml and does not crystallize or separate out within 18 hours.
US20120225914 Treatment of sunburn using analgesics and antihistamines Combination compositions and kits comprising an analgesic and an antihistamine are provided as well as methods of use in treating sunburn.
WO2013008044A1 Synthesis of (+) and (-) 1 -(5,5-diphenyltetrahydrofuran-3- yl)-n,n-dimethylmethanamine, (+) and (-) 1-(2,2-diphenyltetrahydrofuran-3-yl)-n,n- dimethylmethanamine and (+) and (-) 1-(2,2- dffhenyltetrahydrofuran-3-yl)-n-metihylmethanamine The current invention covers the synthesis of (+) and (-) l-(5,5-diphenyItetrahydrofuran-3- yl)-N,N-dimethylmethanamine [(±)1] and [(-)1] respectively, including their pharmacologically acceptable acid addition salts. The new products can be synthesized starting from 5,5-diphenyltetrahydrofuran-2(3H)-one (4) after insertion of an aldehyde group in the α-position, reduction to the prochiral 3-(hydroxymethyl)-1, 1-diphenylbutane-1,4-diol (6), chemoenzymatic desymmetrization using the enzyme Amano Lipase PS30, tosylation, intramolecular nucleophilic attack, hydrolysis, reaction with trifluoromethanesulfonic anhydride and substitution by dimethylamine, thus producing (+) 1-(5,5-diphenyl- tetrahydrofuran-3-yl)-N,N-dimethylmethanamine [(+)1]. Protection of the product of the chemoenzymatic desymmetrization with tert-butyldimethylsilyl chloride, hydrolysis, tosylation, intramolecular nucleophilic attack, removal of tert-butyldimethylsilyl group, reaction with trifluoromethanesulfonic anhydride and substitution by dimethylamine produces (-) 1-(5,5-diphenyltetrahydrofuran-3-yl)-N,N-dimethylmethanamine [(-)1]. It also covers the synthesis of (+) and (-) 1-(2,2-diphenyltetrahydrofuran-3-yl)-N,N- dimethylmethanamine [(+)2] and [(-)2] respectively and (+) and (-) 1-(2,2-diphenyl- tetrahydrofuran-3-yl)-N-methylmethanamine \(+)3] and [(-)3] respectively, including their pharmacologically acceptable acid addition salts. The new products can be synthesized either starting from the reduction of 5-oxo-2,2-diphenyltetrahydrofuran-3-carboxylic acid (13) with LiA1H4, followed by the cyclization of the obtained triol (14) under acidic conditions, reaction with 1S-(-) or1R-(+)camphanic chloride, recrystallization, hydrolysis, reaction with trifluoromethanesulfonic anhydride and substitution by dimethylamine or methylamine, or by the reaction of R-(-) or S-(+) Mandelic acid and acetic acid with racemic 1-(2,2-diphenyltetrahydrofuran-3-yl)-N,N-dimethylmethanamine (2), recrystallization, followed by reaction with an aqueous solution of NaOH. The compounds mentioned in the invention present neuroprotective, antiepileptic and antidepressant activity and can be used as therapeutic agents.
CN102172358A Timicosin compound preparation and preparation method and use thereof The invention discloses a Timicosin compound preparation and a preparation method and use thereof, which relate to the field of livestock breeding. The Timicosin compound preparation comprises the following components: Timicosin and Pidotimod. The invention also provides the preparation method and use of the Timicosin compound preparation. The Timicosin compound preparation provided by the invention is simple in composition and high in safety; and the Timicosin and Pidotimod in the compound preparation can produce a synergic effect in body, so that the Timicosin, at a lower use concentration, can reduce the number of the blue ear disease viruses in the bodies of newly borne piglets by inhibiting the blue ear disease virus content in the body of sows and thus improves the immunity in the bodies of the piglets and the indexes of the productivity of the piglets and reduce breeding benefit. The Timicosin compound preparation prepared by the invention can be used for breeding sows in a pregnant or lactation period. In addition, the preparation method provided by the invention is simple, and the prepared Timicosin compound preparation is stable.
EP1148871B1 Core tablet for controlled release of gliclazide after oral administration The invention concerns a core tablet for the controlled release of gliclazide which ensures continuous and constant release of the active principle, unaffected by the dissolving medium pH variations, after oral administration.
CN101406567A Medicament for oral cavity for treating dentalgia The invention discloses a buccal drug for treating toothache. The formula of the drug is prepared from the following drugs in weight portions: 9 portions of datura flower, 10 portions of rhododendron lutescens franch, 18 portions of pepper, 15 portions of clove, 18 portions of angelica dahurica, 20 portions of murraya jasminorage, 12 portions of speranskia tuberculata and 6 portions of borneol. The buccal drug has the advantages of relieving pain immediately, recrudescing uneasily after healing and having no side effect; a slight patient can be healed once; and a serious patient can be healed after treating for two to three times. The effective rate is 100 percent; and the cure rate is over 99 percent.
CN1615825A Poly unit slow release preparation The poly unit slow release preparation can reduce the daily times of taking medicine, has active component erythromycin derivative, and consists of several micro pills with at least a kind of erythromycin derivative and at least one kind of organic carboxylic acid in the micro pill core. Permeable membrane coats the pill core to constitute micro pill, and the permeable membrane contains water insoluble polymer for medicine to permeate, water soluble polymer. The erythromycin derivative is preferably clarithromycin.
EP1365761B1 Therapeutic combination of amlodipine and benazepril The present invention especially relates to the use of a combination comprising (1) an ACEI selected from the group consisting of benazepril, benazeprilat, and pharmaceutically acceptable salts thereof, and (2) amlodipine or pharmaceutically acceptable salt thereof, for the manufacture a medicament for the treatment or prevention or delay of progression of a condition selected from the group consisting of hypertension, congestive heart failure, angina, myocardial infarction, artherosclerosis, diabetic nephropathy, diabetic cardiac myopathy, renal insufficiency, peripheral vascular disease, left ventricular hypertrophy, cognitive dysfunction, blood pressure-related cerebrovasular disease, stroke, pulmonary disease or pulmonary hypertension and headache; wherein (i) the amount of amlodipine or a phamaceutically acceptable salt thereof corresponds to 6 mg to 40 mg of the free base and (ii) the amount of the ACE inhibitor or a pharmaceutically thereof corresponds to 20 mg to 160 mg of benazepril hydrochloride.
US20080207625 Synthesis and Purification of Pteroic Acid and Conjugates Thereof Methods for purifying pteroic acid, analogs of pteroic acid, and derivatives of pteroic acid are described. Methods for synthesizing and purifying conjugates of vitamins, including FITC conjugates of folic acid, folic acid analogs, and derivatives of folic acid and folic acid analogs are also described. Purified forms of pteroic acid, derivatives and analogs of pteroic acid, and conjugates thereof are also described.
US20060159790 Composition for preventing or treating dementia comprising a hydroxycinnamic acid derivative or an extract of a plant of genus angelicae containing same A composition for preventing or treating dementia comprising a hydroxycinnamic acid derivative of formula (I), decursinol, a pharmaceutically acceptable salt thereof or an extract of a plant of genus Angelicae containing same, wherein, R1 is H or CH3, R2 is —CH═CHCOOH or formula (a).
US20090012017 Polypeptide Complex that Regulates Cell Cycle and Anergy An active ubiquitin E3 ligase, GRAIL, is crucial in the induction of anergy in cells of the immune system, and in the regulation of cellular proliferation. GRAIL is shown to associate with, and be regulated by Otubain isoforms, including OTUBAIN-1 (DOG, the Destabilizer of GRAIL) and an alternative reading frame splice variant of OTUBAIN-1 (SOG, the Stabilizer of GRAIL). These proteins play opposing roles in the regulation of GRAIL auto-ubiquitination and consequently on its ability to induce anergy and regulate cellular proliferation. DOG serves as an adaptor protein, recruiting the DUB USP8. One major substrate for USP8 is the Ras exchange factor Ras-GRF1, and this protein can be found in a complex with USP8 and GRAIL, which complex is ubiquitinated by GRAIL.
US20100093613 Methods for identifying agents and their use for the prevention or stabilization of fibrosis Agents that stabilize and/or prevent fibrosis are identified by assaying test agents in a battery of assays to measure the effect of the test agent on matrix deposition and remodeling, epithelial health, and inflammation. Treatment for fibrosis is provided using compositions of the invention.
US20050220900 Use of extracts containing phytoestrogen selectively modulating estrogen-receptor-beta The present invention relates to the use of phytoestrogen-containing extracts that selectively modulate estrogen receptor beta (ER-beta) without producing any uterotropic effect, for the treatment of clinical situations and pathophysiological conditions that are selected from the group consisting of: Obesity and thereby to possibly influence the metabolic syndrome, particularly hypertension, asterosclerosis, cardiac infarct, hyperandrogenemia; Menopausal continence disorders; Menopausal heat surges associated with hyperstimulation of the hypothalamic gonadotropin releasing hormone pulse generator; steroid hormonal synthesis disorder, particularly that of progesterone synthesis of the human corpus luteum, resulting in luteal insuffeciency; Alzheimer's disease associated with elevated expression of estrogen receptor beta in hippocampal neurons.
WO2008001389A2 Female contraceptive for transcervical delivery and its' preparation A female contraceptive for transcervical approach consisting of a chemical complex of iodine, itaconic acid and methyl methacrylate in a solvent is provided. Further, a process for preparation of female contraceptive for transcervical approach comprising complexing solution of itaconic acid-methyl methacrylate copolymer comprising itaconic acid and methyl methacrylate in a ratio varying from about 1:3 to about 1:8 respectively with solution of iodine to produce chemical complex of iodine, itaconic acid and methyl methacrylate is also provided.
CN102872085A Application of Houttuynoid A in medicines for treating breast cancer The invention discloses an application of Houttuynoid A in preparing medicines for treating breast cancer, and belongs to the technical field of new applications of medicines. In vitro MTT (Methyl Thiazolyl Tetrazolium) antineoplastic activity evaluation finds that Houttuynoid A has remarkable inhibition effect on the growth of human breast cancer cell lines 4T1, MCF-7, MDA-MB-231 and MCF-7B, so that Houttuynoid A can be used for preparing medicines for inhibiting breast cancer and has good development application prospect. The application of Houttuynoid A in medicines for treating breast cancer is disclosed for the first time, and has extremely high inhibitory activity to breast caner cells as the skeleton type belongs to a completely novel skeleton type.
EP1824837A1 Substituted n-sulfonylaminobenzyl-2-phenoxy acetamide compounds This invention provides a compound of the formula (I): wherein R1 represents a (C1,-C6)alkyl group; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1-C6) alkyl group or a (C1-C6) alkoxy group; R3, R4, R5 and R6 each independently represents a hydrogen atom, a (C1-C6) alkyl, or a halogen atom; R7 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1-C6) alkyl group optionally substituted with a piperidino group, a (C1-C6)alkoxy group optionally substituted with a 3-7 membered cycloalkyl ring, a hydroxy(C1-C6)alkoxy group, a (C1-C8)alkoxy- (C1-C8)alkyl group, a (C1-C6)alkoxy-(C1-C6)alkoxy group, a halo (C1-C6)alkyl group, a (C1-C6)alkylthio group, a (C1-C6)alkylsulfinyl group or a (C1-C6)alkylsulfonyl group; R8 represents a (C1-C6)alkyl group, a halo(C1-C6,)aIkyl group, a (C1-C6)alkoxy group, a hydroxy(C1-C6)alkoxy group, a (C1-C6)alkoxy-(C1-C6)alkyl group or a (C1-C6)alkoxy-(C1-C6)alkoxy group; or R7 and R8, when adjacent to each other, taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents selected from the group consisting of a hydroxy group, a (C1-C6)alkyl group, a (C1-C6)alkoxy group and a hydroxy(C1-C6)alkyl group; and R9 represents a hydrogen atom or a halogen atom; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor, such as pain or the like in mammalian. The present invention also provides a pharmaceutical composition comprising the compound of formula (I).
US20120003244 Methods for apcdd1 mediated regulation of hair growth and pigmentation and mutants thereof The invention provides for methods for controlling hair growth by administering an APCDD1 modulating compound to a subject. The invention further provides for a method for screening compounds that bind to and modulate APCDD1.
WO2011047639A1 Pharmaceutical solution of taxanes comprising chelating agent and preparation method thereof A pharmaceutical solution of taxanes, its preparation method, a composition comprising said solution and its pharmaceutical combination package are disclosed. Said pharmaceutical solution comprises taxanes, a chelating agent and a solvent.
US7125862 Porphyrin-metal complexes and oxygen infusions containing the same A porphyrin metal complex that can form a stable oxygen complex and acts effectively as an oxygen infusion, which comprises: a transition metal ion M of period 4 or 5 coordinating to a porphyrin derivative represented by the following general wherein R1 is an alicyclic hydrocarbon group which may contain a substituent, R2 is an alkylene group and R3 is a group which does not hinder the coordination of an imidazolyl group to M.
CN102125579B Novel application of 5-bit modified 2'deoxycytidine derivative or phosphate thereof in the preparation of medicaments The invention discloses application of a 5-bit modified 2'deoxycytidine analogue or phosphate thereof in the preparation of medicaments for treating cancers. The 5-bit modified 2' deoxycytidine analogue or the phosphate thereof can also be used in combination with deoxythymidine or phosphate thereof to form a medicinal composition for treating tumors. A 5-bit modified 2' deoxycytidine derivative is added with an appropriate amount of thymidine or 5' monophosphate when administrated, so that the toxicity to normal cells is greatly reduced to keep the effect of inhibiting tumor cell proliferation.
WO2012043577A1 Reversing agent for anticoagulants The problem addressed by the present invention is the provision of: a reversing agent that reverses the anticoagulant effects of an FXa inhibitor; and/or a reversal method using said reversing agent. [Solution] A reversing agent for an oral anticoagulant, said reversing agent causing clotting. Said clotting agent is one or more of the following: a dried complex that has the effect of circumventing antibodies for a human blood coagulation factor; a dried complex of human blood coagulation factor IX; and recombinant activated factor VII.
CN102675286A Indazoles compound, and preparation method and application thereof, and medical composition The invention provides indazoles compound shown in a formula (I), stereoisomers, tautomers, solvates, prodrug form, N-oxide and pharmaceutically acceptable salts of the indazoles compound, and a preparation method of the indazoles compound and a medical composition comprising the compounds. The compounds can inhibit the PI3K activity, so that the compounds can be used for treatment of diseases such as cancers, immunological diseases, cardiovascular diseases, inflammation, metabolism/endocrine dysfunction and neurologic diseases, wherein the diseases are caused by functions of abnormal cell survival, multiplication, differentiation, apoptosis and the like related to PI3K.
US20120202865 Substituted-aryl-(imidazole)-methyl)-phenyl compounds as subtype selective modulators of alpha 2b and/or alpha 2c adrenergic receptors A compound having selective modulating activity at the alpha 2B and or alpha 2C adrenergic receptor subtypes is represented by the general Formula 1: wherein R1-R6 is independently selected from the group consisting of H, C1-6 alkyl, halogen, CH2OH, CH2N(R7)2, CH2CN, C(O)R8, CF3, and aryl; wherein R7 is H or C1-6 alkyl; and R8 is H, C1-6 alkyl or aryl. The compounds of Formula 1 can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.
EP1904500A1 New derivatives of heptaazaphenalene, methods for obtaining them, and their use as protecting agents against uv radiation The present invention relates to new heptaazaphenalene derivatives of general Formula (I) and to methods for obtaining them. The physicochemical properties of said compounds allow them to be used as UV radiation absorbents.
CA2758005A1 Methods of treating cancers with her3 antisense oligonucleotides One aspect of the invention provides methods for treating cancers which are resistant to treatment with a protein tyrosine kinase inhibitor by co-treatment with the protein tyrosine kinase inhibitor and one or more antisense oligomers that reduce the expression of HER3 and/or HER2 and/or EGFR. Another aspect of the invention provides methods for treating cancers by co-treatment with an inhibitor of HER2 and one or more antisense oligomers that reduce the expression of HER3.
US7230016 Pioglitazone salts, such as pioglitazone sulfate, and pharmaceutical compositions and processes using the same Water-soluble salts of pioglitazone especially pioglitazone sulfate are useful in pharmaceutical applications.
CN102038736A Mouthwash formula for treating toothache and preparation method thereof The invention relates to a mouthwash formula for treating toothache, which consists of 25-35% of mater convolvulus root, 30-40% of vinegar and 30-40% of water by weight percentage. The preparation method thereof comprises the steps of decocting the 25-35wt% of mater convolvulus root, 30-40wt% of vinegar and 30-40wt% of water together for 15-20 minutes; filtering and removing the dregs. The mouthwash formula cooled can be used to wash mouth frequently and has the advantages of less expenses and convenience.
US20100098788 Extracts of Curcuma and Methods of Use Thereof The present invention relates in part to turmeric extracts that are useful for treating or preventing neurodegenerative disorders. Another aspect of the invention relates in part to turmeric extracts that are useful for treating or preventing inflammatory disorders. In some embodiments, the extracts comprise at least one compound selected from the group consisting of 25 to 500 μg bamosamine, 25 to 750 μg echinaxanthol, 100 to 3,000 μg bisdemethoxycurcumin, 50 to 500 μg daphniyunnine E and 500 to 75,000 μg curcumin per 100 mg of extract. Another aspect of the invention relates to pharmaceutical compositions comprising the aforementioned extracts. Another aspect of the invention relates to methods of treating or preventing neurodegenerative disorders comprising administering to a subject in need thereof an effective amount of the aforementioned extracts or compositions. Another aspect of the invention relates to methods of making the aforementioned extracts.
US20110218241 Antiviral epicatechins, epicatechin oligomers, or thiolated epicatechins from theobroma cacao for treatment of genital warts Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins are applied (A) directly to a genital wart in the form of a cream, ointment, paste or solution, (B) directly to the genital wart wherein such cream, ointment, paste or solution contains as an additional active ingredient a skin permeabilizing agent, (C) following electrosurgical resection or removal of the genital wart in such form of a cream, ointment, paste or solution, (D) following chemical resection or extirpation of the genital wart in such form, (E) following surgical resection or removal of the genital wart in such form, wherein said Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins both provide antiviral activity against multiple strains of human papilloma virus (HPV) and promote healing following resection polymers contained in a vehicle. Disclosed are the compositions, therapeutical kits containing such composition, methods of treatment using such composition, and methods of enhancing the stability of such composition.
CN102488688A Ophthalmic preparation by taking fibrauretinumrecisapierre as main drug The invention relates to an ophthalmic preparation by taking fibrauretinumrecisapierre as a main drug. The ophthalmic preparation prepared by the fibrauretinumrecisapierre comprises eye drops, oculentum, ophthalmic liposome, inclusion compound eye drops and the like through the following steps of: taking the fibrauretinumrecisapierre as an active ingredient and adding minor ingredients for the ophthalmic preparation; and contains the raw components in weight ratio: 0.01-2 percent of fibrauretinumrecisapierre, and the balance of the minor ingredients for the ophthalmic preparation. The experiment results prove that the ophthalmic preparation cannot cause irritant inflammatory reaction, and has better inhibiting effect on conjunctivitis and better stability.
WO2010069138A1 Oryzanol composition and preparation method thereof The present invention discloses a pharmaceutical composition containing oryzanol, phospholipids, cholic acids and/or salts thereof. The water-solubility and the stability of oryzanol have been effectively improved by being prepared into said pharmaceutical composition, the particle diameter and the stability of the said pharmaceutical composition are superior to that of the existing products as well. The present invention also provides an injectable fluid and lyophilized powder of said pharmaceutical composition as well as the preparation method thereof.
EP1696909A1 Benzothiazole derivatives for the treatment of diabetes The present invention is related to the use of benzothiazole derivatives for the manufacture of a medicament for the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) Formula (I). G is an unsubstituted or substituted pyrimidinyl group. L is an unsubstituted or substituted C1-C6-alkoxy, or an amino group, or an unsubstituted or a substituted 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S (e.g. a piperazine, a piperidine, a morpholine, a pyrrolidine). R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C2-C6-alkenyl, unsubstituted or substituted C2-C6-alkynyl or C1-C6-alkoxy, unsubstituted or substituted aryl, halogen, cyano or hydroxy.
EP2125851A2 Erythromycin-based macrolides The invention relates to compounds of Formula (I) wherein R1, R2, and X are as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of Formula (I).
WO2012082765A3 Methods for decreasing body weight and treating diabetes Disclosed herein are methods of treating diabetes (e.g., increasing glucose tolerance, reducing insulin resistance, and decreasing serum lipids) and/or reducing body weight (e.g., treating overweight or obesity) including administering a therapeutically effective amount of a composition including an inhibitor of hypoxia- inducible factor la (HIF1α) to a subject with diabetes or a subject in need of reduction of body weight. The HIF1α inhibitor can be administered in combination with a pharmaceutically acceptable carrier. In some examples, the HIF1α inhibitor is administered orally.
WO2006051314A8 Guanidine derivatives as inhibitors of ddah Compounds of formula (I) have been found to be useful as inhibitors of DDAH. The present invention thus provides the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the treatment of a disease whose pathology is affected by DDAH.
CN1583750A Use of 2-3-methylen-dioxy dibenzo [a, g] quinolizine onium chloride in treatment of diabete The present invention discloses a compound 2,3-methenedioxy dibenzo [a,g] quinolizonium chloride, which compound has the effect of reducing blood sugar, whose structure is presented by the following formulae. And the use of this compound 2,3-methenedioxy dibenzo [a,g] quinolizonium chloride in preparing anti-diabetes drugs is also demonstrated.
CN101766599A Drug combination preparation containing qidimacrin or medicinal composites thereof The invention relates to a drug combination preparation containing qidimacrin or medicinal composites thereof. The technical scheme adopted by the invention is as follows: the drug combination preparation is prepared from qidimacrin having the structure as shown in Formula (1) or a medicinal composite thereof having the structure as shown in Formula (II) as the effective component, and a pharmaceutically acceptable drug carrier, wherein the drug combination preparation can be in any pharmaceutical form of drug. The invention further discloses the application of the drug combination preparation in treating liver cancer, lung cancer and other tumors.
US20050014938 Phenyl substituted triazoles and their use as selective inhibitors of akl5 kinase Phenyl substituted triazoles of formula (I) wherein R1 is naphthyl or phenyl optionally substituted with one or more substituents selected from halo, —O—C1-6alkyl, —S—C1-6alkyl, C1-6alkyl, C1-6haloalkyl, —O—(CH2)n-Ph, —S—(CH2)n-Ph, cyano, phenyl, and CO2R, wherein R is hydrogen or C1-6alkyl, and n is 0, 1, 2 or 3; or R1 is phenyl or pyridyl fused with an aromatic or non-aromatic cyclic ring of 5-7 members wherein said cyclic ring optionally contains up to three heteroatoms, independently selected from N, O and S, and N may be further optionally substituted by C1-6 alkyl, and wherein the cyclic ring may be optionally substituted by ═O; R2 and R3 are independently selected from H, C1-6alkyl, C1-6alkoxy, phenyl, NH(CH2)n-Ph, NH—C1-6alkyl, halo, alkoxy, CN, NO2, CONHR and SO2NHR; two of X1, X2 and X3 are N and the other is NR4 wherein R4 is hydrogen, C1-6alkyl, C3-7cycloalkyl, —(CH2)p—CN, —(CH2)p—CO2H, —(CH2)p—CONHR5R6, —(CH2)pCOR5, —(CH2)q(CR7)2, —(CH2)pOR5, (CH2)qCH═CH—CN, —(CH2)q—CH═CH—CO2H, —(CH2)p—CH═CH—CONHR5R6, —(CH2)pNHCOR8 or —(CH2)pNR9R10; R5 and R6 are independently hydrogen or C1-6alkyl; R7 is C1-6alkyl; R8 is C1-7alkyl, or optionally substituted aryl, heteroaryl, arylC1-6alkyl or heteroaryl C1-6alkyl; R9 and R10 are independently selected from hydrogen, C1-6alkyl, aryl and arylC1-6alkyl; p is 0-4; and q is 1-4 and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.
CA2303177C Taste masked pharmaceutical compositions The present invention discloses the taste masking of drugs by wet granulating the drug with a microcrystaline cellulose compositions then spheronizing the granulation into spheres having a smooth uniform surface and a particle size in the range of 1 to 1000 microns.
CN102512439A Ginseng oligosaccharide composition as well as preparation method and application thereof The invention discloses a ginseng oligosaccharide composition as well as a preparation method and application thereof. The monosaccharide formation of oligosaccharide contained in the ginseng oligosaccharide composition is glucose; and moreover, the molecular weight of the contained oligosaccharide is distributed within a range of 360 to 2,000. The preparation method of the ginseng oligosaccharide composition comprises the following steps of: (a) pulverizing dried ginseng; (b) extracting by using distilled water under the condition of 70 DEG C, repeating for 3 times under the same condition, merging extract at the three times, decompressing, concentrating, freezing and drying; (c) adding 95 percent of ethanol into powder after freezing and drying in the step (b), soaking, centrifugalizing, repeating the operation on residues and volatilizing the ethanol at normal temperature so as to obtain the residues; and (d) redissolving the residues obtained in the step (c) into the distilled water, dialyzing by using a membrane with the trapping molecular weight of 3,000, freezing and drying so as to obtain the ginseng oligosaccharide composition. The ginseng oligosaccharide composition disclosed by the invention has favorable immune activating action to the lymphocytes and the macrophages of a rat in vitro.
CN101142198B Isoxazole combretastatin derivatives for the treatment of disorders The invention relates to compounds of structural formula (I); or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
US20070032474 Use of a compound of formula 1 for making a pharmaceutical composition The invention relates to a compound of formula I or pharmaceutically acceptable salts thereof. The invention further relates to methods of use of this compound.
US20110224284 Putative tumor suppressor microrna-101 modulates the cancer epigenome by repressing the polycomb group protein ezh2 The present invention relates in general to microRNA profiling in disease. More specifically, the invention provides for methods and compositions of microRNA to inhibit the growth and formation of tumors.
CN101732285A Capsule of Acipimox The invention belongs to the field of medicines, particularly relates to an Acipimox slowly-released capsule. The Acipimox slowly-released capsule contains quick-acting small pills, intermediate-acting small pills and long-acting small pills, and the three small pills all contain medicine-carrying pellets; wherein the medicine-carrying pellets contain celphere, Acipimox and a caking agent; preferably, the medicine-carrying pellets comprise the celphere, the Acipimox, the caking agent and a plasticizer. The Acipimox slowly-released capsule fast develops the curative effect after being taken and releases medicines lasting within 12 hours, thereby maintaining more stable blood concentration and longer action time and having the characteristics of small toxic and side effects and more convenient taking.
CN103536532A Alprostadil composition as well as preparation method thereof The invention relates to an alprostadil composition which comprises alprostadil, oil for injection, phospholipid and water for injection, wherein the concentration of alprostadil in the formula is 6-11 micrograms/ml, preferably 7-9 micrograms/ml, the concentration of oil for injection is 100mg/ml and the concentration of phospholipid is 18mg/ml. The encapsulation efficiency of the alprostadil injection prepared by the invention is over 95%.
CN102911193A Zinc complex of 2-bromobenzaldehyde hydrazino sulfo-benzyl formate Schiff base and application thereof The invention disclose a metal complex of 2-substituted benzaldehyde hydrazino dithio-benzyl formate Schiff base and an application thereof, belonging to the fields of bioinorganic chemistry. The complex has the structure as shown in the specification.
US20080171081 Administering liposomes carrying phosphate-glycerol groups; inhibiting and/or reducing the progression of the T-cell function-mediated disorder; antiinflammatory This invention relates to three-dimensional synthetic and semi-synthetic compositions having biological activity, and to the uses thereof in the treatment and/or prophylaxis of various disorders in mammalian patients. More particularly it relates to preparations and uses of synthetic and semi-synthetic bodies, such as liposomes, which after introduction into the body of a patient, produce beneficial anti-inflammatory, organ protective and immune regulatory effects. The invention also relates to treatments and compositions for alleviating inflammatory and autoimmune diseases and their symptoms.
CN103083472A Nano silver anti-inflammatory gel for treating gynecologic inflammation and preparation method thereof The invention discloses a nano silver anti-inflammatory gel for treating gynecologic inflammation and a preparation method thereof. The gynecologic inflammation is a common frequently-occurring disease; and an ideal effect cannot be easily obtained from the traditional therapeutic drug. 1000g of gel is prepared from 100-200 PPM of nano silver powder, 2-3g of camellia oil, 2-3g of eucalyptus oil, 0.002-0.008g of sodium dodecyl sulfate, 10-20g of propolis, 4-6g of carbopol, 4-6g of triethanolamine and the balance of pure water. The nano silver anti-inflammatory gel has excellent curative effect on pathogenic microorganism infective inflammation diseases such as gynecologic inflammation, cervicitis, or mixed infection. The gel disclosed by the invention is directly administered through vagina; and the drug directly achieves the focus of infection, and is explicit in targeting property, concise and convenient. The nano silver anti-inflammatory gel has strong inhibiting or killing roles on various pathogens such as gram positive bacteria, gram negative bacteria, mould, trichomonad and the like by experimental and clinical validation. The nano silver anti-inflammatory gel has good curative effect on colpitis, cervicitis, annexitis and pelvic inflammation caused by lactobacillus, mycete, candida albicans, HPV (human papillomavirus) and the like.
CN103536601A Preparation method of medicine used for controlling pasteurella infection of livestock and poultry The invention relates to compound sulfachlorpyridazine sodium powder, and specifically provides a preparation method of compound sulfachlorpyridazine sodium powder used for controlling pasteurella infection of livestock and poultry. 100 parts of the compound sulfachlorpyridazine sodium powder comprise 60 to 65 parts of sulfachlorpyridazine sodium, 2 to 4 parts of indometacin potassium, 10 to 25 parts of a suspending agent, 2 to 4 parts of a corrigent and the balance an acceptable carrier. The ingredients above are mixed and grinded so as to obtain the compound sulfachlorpyridazine sodium powder. The compound sulfachlorpyridazine sodium powder possesses accurate curative effects on pasteurellosis of a plurality of animals, and is suitable for popularization and application in livestock breeding. According to the preparation method, sulfachlorpyridazine sodium and indometacin potassium are used together, besides antisepsis and anti-inflammation effects, indometacin potassium is used as an antibacterial synergist of sulfachlorpyridazine sodium, so that synergistic effect is achieved, and pharmacological function of the main medicine is improved. Absorptivity of the compound sulfachlorpyridazine sodium powder, which can be taken orally, or mixed with feed for use, or dissolved in drinking water for use, is high; drug tolerance is difficult to be caused; the compound sulfachlorpyridazine sodium powder is safe to be used for protection, prevention and therapy in a long term. Palatability, fluidity and suspending water solubility are excellent; clinical administration methods are diverse; and the compound sulfachlorpyridazine sodium powder is convenient for clinical administration.
US20070021330 cyclic peptides used as enzyme inhibitors, optionally mixed with carriers or excipients, and viricides selected from interferons, ribavirin and amantadine, for treatment of viral diseases The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt, ester, or prodrug, thereof, which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
CN1911241A Slow-released type iodine complement agent, and prepn. method and use-thereof A slow-release I-supplement used as the I-supplementing additive of forage or to prepare I-supplementing food or medicine for treating diseases is an anionic exchange resin containing the iodic acid radicals or I ions. It is prepared through the ionic exchange between iodic acid radicals or I ions and anionic exchange resin.
WO2013147135A1 Controlled-release pharmaceutical composition Provided is a controlled-release pharmaceutical composition which contains 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]- amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, which is a compound of which the solubility in an acidic pH region is extremely different from that in a neutral pH region, as a medicinal agent, wherein the solubility of the medicinal agent can be maintained in a neutral pH region in the digestive tract after gastric emptying (e.g., the small intestine) and the controlled-release pharmaceutical composition exhibits a good oral absorption property and has high bioavailability. The controlled-release pharmaceutical composition comprises 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H- pyrrolo[2,3-b]pyridine-5-carboxamide or a pharmaceutically acceptable salt thereof, an acidic substance, a persaturation-maintaining agent, and a controlled-release base ingredient.
CN101579416B Orthopedics plaster The invention discloses an orthopedics plaster and a preparation method thereof. The orthopedics plaster comprises the following components by weight portion: 10 to 30 portions of drynaria, 10 to 30 portions of lycopodium clavatum, 10 to 30 portions of safflower, 10 to 30 portions of angelica, 10 to 30 portions of folium cortex eucommiae, 10 to 30 portions of teasel root, 10 to 30 portions of gecko, 10 to 30 portions of processed semen strychni, 10 to 30 portions of herba pyrolae, 10 to 30 portions of fructus liquidambaris, 10 to 30 portions of tinospora sinensis, 10 to 30 portions of radix clematidis, 10 to 30 portions of rhizoma atractylodis, 10 to 30 portions of spatholobus stem, 10 to 30 portions of rhizoma ligustici wallichii, 10 to 30 portions of achyranthes, 10 to 30 portions of myrrh, 10 to 30 portions of frankincense, 10 to 30 portions of cassia twig, 10 to 30 portions of notopterygium, 10 to 30 portions of scorpion, and 10 to 30 portions of borneol. The plaster is applied tothe surface of skin and gives play to the functions of clearing and activating channels and collaterals, opening orifices penetrating bones, and dispelling wind and dissipating cold of medicaments, can ease and rehabilitate rheumatism, hyperosteogeny, lumbar muscle strain and pains caused by bruises, and has rapid medicament action and outstanding curative effect.
CN103690778A Synthetic type breast-beautifying medicine for external use and preparation method thereof The invention relates to the field of medicinal preparations about animal and plant materials, and in particular to a synthetic type breast-beautifying medicine for external use and a preparation method of the medicine. The synthetic type breast-beautifying medicine comprises the following ingredients in parts by weight: 280-320 parts of radix astragali, 170-190 parts of red ginseng, 110-130 parts of white atractylodes rhizome, 85-95 parts of angelica sinensis, 110-130 parts of white peony root, 115-125 parts of root of Chinese trichosanthes, 70-75 parts of platycodon grandiflorum, 170-190 parts of root of red-rooted salvia, 140-160 parts of motherwort, 85-95 parts of rhizoma cyperi, 85-95 parts of tuckahoe, 170-190 parts of radix ophiopogonis, 58-62 parts of liquorice, 140-160 parts of pearl powder, and 90-110 parts of gypsum powder. The raw materials are socked, decocted, heated and concentrated to be pasty, and then mixed with medicinal vaseline and vegetable fat uniformly to obtain the synthetic type breast-beautifying medicine for external use.
US20120219615 Therapeutic Use of a TLR Agonist and Combination Therapy The present invention is directed generally to formulations of a TLR agonist preferably a TLR8 agonist, and its use in the treatment of various diseases, including combination therapies for treating cancer.
US20130053333 Aminoquinoline Derivatives This invention relates to novel aminoquinoline derivatives of Formula (I) or Ia, or pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an aminoquinoline derivative, such as a derivative of primaquine.
US20110064774 Bulking agent The invention relates to bulking agents and apparatus and methods for using the disclosed bulking agents. The bulking agents can be used to treat such conditions as urinary and fecal incontinence, gastro-esophageal reflux, aneurismal blockages, and cosmetic deformities. The invention also relates to an injection method that reduces the injection pressure required to place the bulking agents.
US20090221716 Composition Comprising At Least 3 Different Diols The present invention relates to a composition comprising at least 3 different diols, wherein said diols have the general structure (CH2)nH2O2, wherein n is the number of CH2 and being between 3 to 10, in a total amount of from about 0.1 to about 50% (v/v), a method for producing the composition and its use, such as in therapy. The composition may be a pharmaceutical, cosmetic, antimicrobial or preservative composition. The composition is useful in inactivating microorganisms or preventing their growth.
CA2427388C Pharmaceutical compositions and uses for improving memory and learning impairments The present invention makes available methods and reagents for enhancing and/or restoring long-term memory function and performance, e.g., to improve long-term memory (LTM) and recall ability in animal subjects.
CN103417547A Applications of medicine prepared from ceftriaxone and used for curing and/or preventing dementia caused by Parkinson's disease The invention discloses applications of medicine prepared from ceftriaxone and used for curing and/or preventing dementia caused by Parkinson's disease.
US20080064697 Antidiabetic agents; somatostatin receptor subtype 5 modulators; noninsulin dependent diabetes mellitus; side effect reduction; synthesis This invention is concerned with compounds of the formula wherein A, R1 to R5 are as defined in the specification and G is a pyridine, quinoline or pyrimidine group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
WO2007098520A1 Process for the manufacture of a composition containing at least one xanthophyll The present invention relates to a process for the manufacture of a composition containing at least one xantophyll selected from the group consisting of lutein and zeaxanthin, said process comprising the steps of: providing an extract of Marigold flower containing the xantophyll(s) in esterified form; saponifying the Marigold flower extract and isolating the xantophyll(s). The process according to the invention is characterized in that the step of saponifying the Marigold flower extract is carried out in the presence of a quaternary ammonium base.
CN102895484A Compound injection for clearing away heat and toxic materials and preparation method thereof The invention discloses a compound injection for clearing away heat and toxic materials and a preparation method thereof. The injection is mainly prepared from the following bulk pharmaceuticals by weight: 650-700g of gypsum, 65-70g of weeping forsythia, 120-140g of honeysuckle flower, 65-70g of fructus gardenia, 70-90g of rehmannia root, 65-70g of philippine violet herb, 100-110g of figwort, 65-70g of baikal skullcap root, 65-70g of gentian, 50-60g of common anemarrhena, 65-70g of isatis root, 50-60g of dwarf lilyturf root and 50-60g of taurine. The injection has the effects of resisting inflammation, alleviating pain and refrigerating, and can be used for treating flu, lung plague, strangles, upper respiratory tract infection and various febrile diseases.
WO2009071308A1 Pharmaceutical containing a hormone combination having a contraceptive effect and an insulin sensitizer The present invention relates to a pharmaceutical in the form of daily doses, containing an active ingredient combination comprising a hormone combination having a contraceptive effect, consisting of at least one estrogen, selected from the group consisting of estradiol and ethinyl estradiol, and at least one gestagen, selected from the group consisting of chlormadinone acetate, 3-ß-OH-chlormadinone acetate, 3-α-OH-chlormadinone acetate, 3-α-acetoxy-chlormadinone acetate, and 3-ß-acetoxy-chlormadinone acetate, and at least one insulin sensitizer, and which are combined into a pharmaceutical form using daily doses, containing only one insulin sensitizer as the only active ingredient, and to the use of said pharmaceutical form as prophylaxis against, or as a therapy for pathological disorders caused by the polycystic ovarian syndrome (PCOS), and simultaneously for contraception.
CN101352454A External-use gel foamable composition for gynecology inflammation and obesity The invention discloses a gel foaming agent used for treating gynecological inflammation and adiposity through external application. The gel foaming agent is composed of nano silver, weight-reducing medicine, a foaming agent, a transdermal absorption agent and an excipient. The invention describes the characters of the medicine such as formulation composition, preparation technique and disposable packaging. The gel foaming agent for external application can be applied on the skin or mucous membranes and has significant curative effects for treating vaginitis, cervicitis, cervical erosion, mixed infection type gynecological inflammation and adiposity; furthermore, the gel foaming agent for external application has great significance for popularization in industrial production.
WO2014031897A1 Oral dosage forms having a high loading of (n,n- diethylcarbamoyl)methyl methyl|(2e)but-2-ene-1,4-dioate Oral dosage forms and granulations with a high loading of (N,N- Diethylcarbamoyl)methyl methyl (2E)but-2-ene-l,4-dioate are disclosed.
WO2007130821A3 Mglur5 modulators ii The present invention is directed no novel compounds of formula (I), to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds. Formula (I):
EP1939203A2 Inhibitors of human phosphatidyl-inositol 3-kinase delta isoform Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3Kδ isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compound s to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.
US20050080121 for example, 4S-[(naphthalene-2-carbonyl)-amino]-5-(2-oxo-pyrrolidin-3S-yl)-pent-2-enoic acid ethyl ester; treatment of viral infections caused by human rhinoviruses, human polioviruses, human coxsackieviruses, human echoviruses, among others Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.
CN1813724A Liranaftate paste and its preparing method The present invention relates to a rilanaizhi ointment preparation and its preparation method. Its main components contain active effective component rilanaizhi and medicinal matrix, in which the medicinal matrix contains one kind or several kinds of oleaginous matrixes and water-soluble matrixes, also can contain other additives of preservative and surfactant, etc. Besides, said invention also provides its preparation method and concrete steps.
CN103550192A Application of natural compound Magnolol in preparation of medicines for treating tumor migration and invasion The invention discloses application of Magnolol in preparation of medicines for treating breast cancer migration and invasion. The Magnolol has the following characteristics that the transcriptional activity of a transcription factor NF-kB is inhibited, the transcriptional expression of the NF-kB on downstream gene matrix metalloproteinase MMP-9 is inhibited, and then an acceleration function of the enzymatic activity of the MMP-9 on tumor cell migration and invasion is inhibited. The Magnolol has effective anti-tumor proliferation and anti-MMP-9 expression effects in a naked mouse breast cancer subcutaneous load migration tumor model. The Magnolol serves as a natural compound and can overcome an acceleration effect of a chemical carcinogen phorbol ester PMA on tumor invasion. The Magnolol achieves a novel level in targeted therapy aspects of tumor migration and invasion of natural compounds, and has good application prospects.
CN103288790A Preparation method and application of triterpenoid with effect of resisting rheumatoid arthritis The invention relates to a preparation method of isomalabaricane triterpenes (isomalabaricane triterpenes) jaspolide B with strong proliferation activity of inhibiting a human fibroblast-like synovial cell, and application thereof in the treatment aspect of rheumatoid arthritis. The compound is shown in a structural formula 1; the fibroblast-like synovial cell (FLS) of a sufferer with the rheumatoid arthritis (RA) is utilized as a model for evaluating the activity of resisting the rheumatoid arthritis, so as to find out that the jaspolide B has strong proliferation activity of inhibiting the human fibroblast-like synovial cell; the IC50 value is 10 muM. By adopting the preparation method, a lead compound is provided for development of a new drug for resisting the rheumatoid arthritis; development and utilization of the medicinal value of marine sponge are facilitated.
US7662830 2-{4-[6-(3-Chloro-4-fluoro-phenyl)-2-morpholin-4-yl-pyrimidin-4-yl]-piperazin-1-yl}-nicotinic acid ethyl ester; 5-Methyl-6-{4-[2-(2-methyl-pyrrolidin-1-yl)-6-phenyl-pyrimidin-4-yl]-piperazin-1-yl}-nicotinic acid; treating conditions related to capsaicin receptor activation; neurophathic pain Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptors activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
US20080119517 Compositions and methods for protecting against mitochondria component-mediated pathology Compositions and methods used for preventing mitochondrial component-based diseases are disclosed herein. In particular, heterocyclic compositions and methods that are directed toward protecting against changes in mitochondrial permeability transition that could result in cell death.
CN102058543A Tramadol-containing controlled-release micropill and preparation method thereof The invention discloses a tramadol-containing controlled-release micropill comprising a medicated micropill and a controlled-release layer. A preparation method of the tramadol-containing controlled-release micropill comprises the following steps of: mixing a hollow pill core wrapped with tramadol or auxiliary materials with medicines to prepare a micropill so as to obtain the medicated micropill; preparing a retardant, a pore-foaming agent and a plasticizer or an antisticking agent into a coating solution, and then spraying on the outer layer of the medicated micropill in a coating pan or a fluidized bed to prepare the tramadol-containing controlled-release micropill. The prepared tramadol-containing controlled-release micropill can effectively control the medicines to be released within certain time and keep effective blood concentration stable without burst release phenomena.
US20090269422 Methods for controlling angiogenesis and cell proliferation The present invention relates generally to methods of inhibiting angiogenesis in a patient by administering an effective angiogenesis-inhibiting amount of a thrombin inhibitor, and to the treatment of disease states that result from uncontrolled cell proliferation by administering a thrombin inhibitor alone or co-administering a thrombin inhibitor with an anticancer or cytotoxic agent. Specifically, the thrombin inhibitors used in the methods of the present invention are hirudins.
US20080020060 Process for treating rhinitis A colloidal suspension comprising elemental silver and/or one or more alloys of silver is mixed with either an over-the-counter rhinitis medicine or a prescription rhinitis medicine. The resulting mixture is administered to rhinitis patients in the form of a spray.
CN102552270A Composition prepared by epigallocatechin gallate and 5-fluorouracil for inhibiting tumor cell proliferation The invention belongs to the field of medicine and genetic engineering and provides a composition for inhibiting tumor cell proliferation. The composition for inhibiting the tumor cell proliferation comprises the following active ingredients: epigallocatechin gallate, 5-fluorouracil as well as necessary auxiliary materials for pharmaceutics, wherein the molar ratio of the epigallocatechin gallate and the 5-fluorouracil is 2.5:1-0.3:1. An experiment confirms that with the adoption of the composition prepared by the epigallocatechin gallate and the 5-fluorouracil or by jointly using the epigallocatechin gallate when the 5-fluorouracil is dosed, the treatment effect of the 5-fluorouracil in inhibiting the tumor cell proliferation can be remarkably treated; no toxicity is generated to nude mice livers and kidneys; the epigallocatechin gallate in the active ingredients is rich in resource and low in price; and while the inhibition ratio of tumor is improved, the treatment cost of tumor patients is reduced.
CN101273971A Ethosomes preparation of antimycotics pharmaceutical and method for preparing the same The invention discloses an ethosome preparation of an antifungal drug, the antifungal drug is packaged in the ethosome and consists of the following components according to weight percentage: 0.1 percent to 5 percent of the antifungal drug; 1 to 8 percent of phospholipid; 0 percent to 0.5 percent of cholesterol; 20 percent to 45 percent of ethanol; 0 to 0.1 percent of antioxidant; 0 percent to 0.5 percent of nonionic surfactant; and 40.9 to 78.9 percent of water. The invention further discloses three preparation method of the ethosome preparation of the antifungal drug. The ethosome preparation of the antifungal drug is characterized by non-irritation for skin, strong transdermal infiltration capability and significant anti-bacterial effect.
WO2008096841A1 Dimerized cyclo derivative [PROBLEMS] To provide a novel dimerized cyclo derivative having excellent DPP-IV inhibitory activity or a pharmacologically acceptable salt thereof, and a prophylactic and/or therapeutic agent for a DPP-IV-related disease which comprises the derivative or the pharmacologically acceptable salt thereof as an active ingredient. [MEANS FOR SOLVING PROBLEMS] Disclosed is a dimerized cyclo derivative represented by the general formula (1) or a pharmacologically acceptable salt thereof (e.g., 1,2-ethanediol bis[4-[2-[(2S,4S)-2-cyano-4- fluoropyrrolidin-1-yl]acetyl]aminobicyclo[2.2.2]octane-1- carboxylate]).
EP1363614B1 Use of 2-amino-1-(4-hydroxy-3-methanesulphonamidophenyl)ethanol for treating urinary incontinence The present invention relates to medicaments containing 2-amino-1-(4-hydroxy-2-methanesulphonamidophenyl)ethanol, one of the two optical isomers thereof and/or the pharmacologically acceptable salts thereof, particularly for treating urinary incontinence
EP1515709A2 Use of an alpha2delta ligand such as gabapentin or pregabalin for treating attention deficit hyperactivity disorder This invention relates to a method of treating ADHD by administering an alpha2delta ligand such as, for example, gabapentin or pregabalin, or a pharmaceutically acceptable salt thereof.
WO2006127057A1 Non-systematic vaginal administration of estrogen and an androgen for the treatment of sexual dysfunction Methods and formulations for treating female sexual dysfunction are provided. A pharmaceutical composition for topical non-systemic administration is formulated so as to contain a selected estrogen and/or androgen agent administered to the vagina, vulvar area of the individual undergoing treatment.
US7731973 Administering estriol to treat multiple sclerosis, autoimmune diseases, psoriasis, Sjogren's syndrome, encephalomyelitis; inflammatory bowel, Crohn's, Hashimoto's, or Addison's disease; diabetes, myasthenia gravis, lupus, rheumatoid arthritis, polymyositis; immunotherapy; magnetic resonance imaging The invention provides a method of ameliorating a Th1-mediated immune pathology in a mammal. The method is practiced by administering a low dose of estrogen to the mammal. Optionally, an immunotherapeutic agent can also be administered to the mammal. Also provided are kits containing a low dose of estrogen and an immunotherapeutic agent.
WO2013027001A1 Compounds and their use to treat histamine h3 related disorders The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, m, n, p, q, Q1, Q2, Q3, Q4, Q5, Q6, X1, X2, X3, X4, A1 and L1, are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
US7795261 substance P receptor blockers, such as [2R-trans]-{2-benzyl-4-[4-(1-pyrazin-2-yl-pyrrolidin-3-yl)-piperazin-1-yl]-piperidin-1-yl}-(3,5-bis-trifluoromethyl-phenyl)-methanone, used for treating schizophrenia, emesis, anxiety and depression, irritable bowel syndrome, sleep disorders, pain and inflammation This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis and IBS. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P and Neurokinin B by blocking the NK1, NK2 and NK3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
CN1663567A Compound menonine and Vitamin B1 freeze-dried injection and its preparation Compound methilanin thiamin is used to assist treat that acute and chronic hepatitis, fatty liver, early cirrhosis of liver, toxic hepatitis brought by arsenic and barbiturate and other diseases in clinic. But, there is only liquid drugs injection supplied in market at present. Compound methilanin thiamin is unstable to heat; thiamin is easy to decompose on condition of solution, opacification or precipitate; after sterilization at high temperature, content of thiamin in liquid drugs injection will decrease for decomposition; meantime the storage and transport for liquid drugs injection is not convenient. The invention overcomes the shortage of methilanin thiamin liquid drugs injection, increases stability of drug, is propitious to transport and storage; and avoids freezing easily in winter and affecting quality of drug, prolongs drug storage life, improves quality of drug, in order to treat patients more safely and effectively.
WO2014100852A1 Inhibition of cancer growth and metastasis The present invention relates to methods for treating or preventing cancer and metastasis. More particularly, the present invention relates to methods for treating or preventing cancer by decreasing the expression and/or activity of Flightless I. Also provided are methods for inhibiting the growth of a cancerous cell and methods for inhibiting formation and/or growth of a tumour which also rely on decreasing the expression and/or activity of Flightless I. The present invention also extends to methods for diagnosing cancer, methods for determining if a subject is susceptible to developing cancer, and methods for assessing progression of cancer based on the finding that increased expression and/or activity of Flightless I is associated with cancer development, growth and metastasis. The present invention also provides methods for screening for a candidate therapeutic agent useful for treating or preventing cancer, and related pharmaceutical compositions and kits.
CN1939275A Oral preparation containing mezlocillin and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains mezlocillin. Its preparing process is also disclosed.
CN102600109A Dexlansoprazole sustained release capsule and preparation method thereof The invention belongs to the technical field of pharmaceutical preparation, and particularly relates to a dexlansoprazole sustained release capsule and a preparation method thereof. Two kinds of pellets are arranged in the capsule, and the weight ratio of dexlansoprazole contained in the first kind of pellets and the second kind of pellets is 1:3-4. The dexlansoprazole sustained release capsule disclosed by the invention can avoid the destruction of the dexlansoprazole in gastric acid, and is released in the intestinal tract in a fixed position so as to achieve the purposes of taking effect rapidly and improving bioavailability.
US20100310500 Alkanoylamino benzamide aniline hdac inhibitor compounds The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
WO2013119774A1 3-(2-amino-ethyl)-alkylidene)-thiazolidine-2,4-dione and 1-(2-amino-ethyl)-alkylidene-1,3-dihydro-indol-2-one derivatives as selective sphingosine kinase 2 inhibitors 3-(2-amino-ethyl)-5-[3-(4-substituted-phenyl)-alkylidene)-thiazolidine-2,4-dione and l-(2-amino-ethyl)-3-alkylidene-l,3-dihydro-indol-2-one and derivatives thereof are provided for use as selective SphK2 inhibitors and for use in the treatment of human diseases, such as cancer.
WO2014021284A1 Anti-trichophytic adhesive patch The present invention provides an adhesive patch for nails and/or skin, which has anti-trichophyton activity and high nail permeability. An adhesive patch for nails and/or skin for prophylaxis or treatment of trichophytosis, which contains a compound represented by general formula (I) or a salt thereof in an adhesive layer. (In the formula, R1 represents a hydrogen atom, a C1-6 alkyl group or a trifluoromethyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, a halogen atom, a -COO(C1-6 alkyl) group or a (CH2)1-3COOR group (wherein R represents a hydrogen atom or a C1-6 alkyl group); R3 represents a hydrogen atom, a C1-6 alkyl group, an amino group, a trifluoromethyl group or an OR group (wherein R represents a hydrogen atom or a C1-6 alkyl group); R4 represents a hydroxyl group; R5 represents a hydrogen atom, a C1-6 alkyl group, a hydroxyl group or a halogen atom; R6 represents a hydrogen atom, a C1-6 alkyl group, a trifluoromethyl group, a halogen atom, an amino group, an -NRaRb group, a nitro group, a hydroxy C1-6 alkyl group, a -CONRaRb group, a -COO(C1-6 alkyl) group, a -COOH group, a -(CH2)1-3COOR group or an ORa group (wherein R represents a hydrogen atom or a C1-6 alkyl group; and Ra and Rb may be the same or different, and each represents a hydrogen atom, a C1-6 alkyl group or a C1-6 acyl group); R7 represents a hydrogen atom, a C1-6 alkyl group, an -OR group (wherein R represents a hydrogen atom or a C1-6 alkyl group) or a halogen atom; and R8 represents a hydrogen atom, a C1-6 alkyl group, a hydroxyl group, an amino group or a nitro group.)
EP1771426B1 Diphenylamine-substituted salicylthiazole derivatives and related compounds as phosphotyrosine phosphatase 1b (ptp1b) inhibitors for using as blood-sugar decreasing active ingredients for treating diabetes The aim of the invention is to provide compounds having a therapeutic blood-sugar decreasing effect. Said compounds are suitable especially for the prevention and treatment of pancreatic diabetes. To this end, the invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5 independently represent H, F, Cl, Br, J, OH, CF3, NO2, CN, OCF3, O-(C1-C6)-alkyl, O-(C1-C4)-alkoxy-(C1-C4)-alkyl, S-(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, O-(C3-C8)-cycloalkyl, (C3-C8)-cycloalkenyl, O-(C3-C8)-cycloalkenyl, (C2-C6)-alkinyl, aryl, O-aryl, (C1-C8)alkylene-aryl, O-(C1-C8)-alkylene-aryl, S-aryl, CO-NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, NH-SO2-CH3, SO2-CH3, COOH, COO-(C1-C6)-alkyl, or CO-N((C1-C6)-alkyl)2; R6 represents H, (C1-C6)-alkyl; A represents a bond, -CH2-, -NH-, -CH2-O-, -S-, -CH2-CH2-, or -CH(CH3)-; B represents NH, NH(C1-C4)-alkyl, or NH(CO); and D represents phenyl or a heterocycle. The invention also relates to the physiologically compatible salts of said compounds.
US20110097373 Bone prosthetic material and method of manufacturing the same A method of manufacturing a bone prosthetic material, includes by forming tricalcium phosphate (TCP) particle precursor particles; by performing preliminary sintering on the TCP precursor particles at a temperature in a first temperature range to produce TCP particles of diameters in a predetermined diameter range; by granulating the TCP particles to produce granulated bodies; and by performing sintering on the granulated bodies at a temperature in a second temperature range to generate sinter assemblies. The second temperature range is higher than the first temperature range. In the bone prosthetic material manufactured thus, a first space in a range of 100 to 400 μm is formed between adjacent two of a plurality of sintered assemblies. Each of the plurality of sintered assemblies includes tricalcium phosphate (TCP) particles which are subjected to sintering, and a second space in a range of 5 to 100 μm is formed between adjacent two of the TCP particles. The second space communicates with the first space. Each of the plurality of sintered assemblies has a connection portion connecting the TCP particles, and the connection portion has a width in a range of 5 to 20 μm.
CN102429903A Ozagrel sodium medicinal composition for injection The invention discloses an ozagrel sodium medicinal composition for injection. Ozagrel sodium injection consists of ozagrel sodium, sodium citrate and calcium disodium edetate, wherein each piece of injection contains 40-100 mg of ozagrel sodium, 4-10 mg of sodium citrate and 0.02-0.05 mg of calcium disodium edentate. A preparation method of the composition comprises the following steps of: adding a prescription dose of sodium citrate and calcium disodium edentate into a prescription dose of 90 percent injection water at the temperature of 55-65 DEG C and stirring to dissolve; adding a prescription dose of ozagrel sodium and stirring until the ozagrel sodium is fully dissolved; measuring an initial pH value, and adjusting the pH value to be within a range of 7.5-9.5 by using 4 percent sodium hydroxide solution and 10 percent sodium citrate solution according to the initial pH value; adding medicinal carbon and stirring; performing extraction filtration, replenishing injection water to full amount and uniformly mixing; performing fine filtration; canning; sterilizing; performing light inspection; and warehousing to obtain the ozagrel sodium injection. The ozagrel sodium medicinal composition has high light stability, clarity and stability and does not produce crystals, and has the more obvious advantages of improving the product yield, reducing the cost, realizing industrialization and guaranteeing better application to clinical use.
EP2563361A1 Boosting immune defense by upregulating ccaat/enhancer binding protein epsilon The present invention demonstrates the important role of C/EBP&egr; in innate immune response against pathogens. Specifically, the inventors showed that in the absence of functional C/EBP&egr;, mice are severely impaired in their ability to clear S. aureus infection. Neutrophils are particularly affected, and susceptibility to S. aureus can be rectified by treatment with interferon-gamma (IFN-γ). Importantly, increased activity of C/EBP&egr;, either by induced overexpression of C/EBPE or by application of nicotinamide or an analog, derivative or salt thereof, dramatically enhances immune killing of S. aureus and leads to amelioration of infection.
CN103142496A Calcitriol controlled-release granule and preparation method thereof The invention relates to a calcitriol controlled-release granule and a preparation method thereof. The controlled-release granule consists of a core and a controlled-release coating layer, wherein the controlled-release coating layer contains an controlled-release material accounting for 10-20% by weight, and the core is prepared from the following ingredients in percentage by weight: 0.002% of calcitriol, 2.0-4.0% of meglumine, 1.2-1.8% of polyethylene glycol 400, 15-25% of polyethylene glycol 6000, 50.0-70.0% of filler, 5.0-10.0% of disintegrant and an appropriate amount of binder. According to the controlled-release granule, the content of calcitriol is remarkably increased, so that the drug dosage is reduced; and the stability of calcitriol to light and air is improved, and the bioavailability of calcitriol is also remarkably improved.
CA2169071C Methods for modulating the human sexual response The invention is directed to improved methods for modulating the human sexual response by administering a vasodilator to the circulation by a route of administration that avoids the "first-pass" effect.
US7598042 Early prostate cancer antigens (EPCA), polynucleotide sequences encoding them, and their use A novel prostate cancer marker is described that is found in cancerous and normal prostate cells of individuals that have prostate cancer but is not found in the prostate of individuals without prostate cancer. The marker also is present in normal tissue adjacent to tumor tissue in individuals having prostate cancer. The marker, however, is absent in the prostate of individuals without prostate cancer. Methods employing the novel prostate cancer marker of the invention to predict the occurrence of the prostate disease, monitor the progression of prostate cancer and effect the treatment of prostate cancer, also are described.
US20090176887 Biocidal Compositions and Methods Biocidal compositions comprises an effective amount of a biocidal agent such as a quaternary ammonium compound or a blend of quaternary ammonium compounds and an effective amount of a cellular membrane disruptor. The synergy index of the biocidal agent and the cellular membrane disruptor is less than 1. The biocidal compositions can further comprise an effective amount of a chemical stabilizer and other optional components such as a nonionic surfactant. Methods for making and utilizing such biocidal compositions are also disclosed.
CN102886047A Baicalein combination and preparation method thereof The invention belongs to the field of pharmacy and relates to a baicalein combination and a preparation method thereof. The novel baicalein combination provided by the invention comprises baicalein, a solid dispersion carrier, a plasticizer and an anti-plastering aid, and is prepared by adopting a hot melting extrusion technology. According to the combination, the preparation process is simple, the industrial mass production is easy to realize, and no organic solvent residuals exist. The prepared combination has the advantages that the stability is good, and the in-vitro dissolution and bioavailability of the baicalein are greatly improved.
US8273734 5HT2C receptor modulators The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
US20070293559 Orally Administered Agent For Preventing Or Improving Dry Station Of Skin Orally administered agents, foods and drinks, feeds, food additives or feed additives for preventing or treating a dry state of the skin accompanied by atopic dermatitis, xeroderma, chapped hand, chapped skin and the like are provided. The present invention can provide orally administered agents, foods and drinks, feeds, food additives or feed additives for preventing or treating a dry state of the skin, which comprise hydroxyproline, an N-acyl derivative of hydroxyproline, especially an N-acetyl derivative, an N-propionyl derivative, an N-butyryl derivative, an N-isobutyryl derivative, or a salt thereof as an active ingredient.
US20120189718 Medicine for dissolving and eliminating wart and excrescence consisting of protein and its uses A pharmaceutical composition for dissolving and eliminating wart and excrescence consisting of protein is disclosed in the present invention. The pharmaceutical composition comprises (in 100 weight parts) 1.0-60.0 parts of sodium hydroxide and/or potassium hydroxide. The pharmaceutical composition further comprises 0.25-1.0 parts of tetracaine, bufalin, venenum bufonis and/or menthol having local anesthetic effect. The pharmaceutical composition can dissolve and eliminate wart and excrescence consisting of protein immediately and has significant effect and low side effect.
CN102860995A Enrofloxacin effervescent granule for livestock and preparation method thereof The invention relates to an enrofloxacin effervescent granule for livestock and a preparation method of the enrofloxacin effervescent granule. The enrofloxacin effervescent granule comprises the following raw materials and auxiliary materials in parts by weight: 80-120 parts of enrofloxacin, 100-140 parts of citric acid, 150-170 parts of sodium bicarbonate, 20-40 parts of polyethylene glycol 6000, 190-260 parts of dextrin and 310-390 parts of cane sugar. The preparation method comprises the steps of respectively crushing the raw materials and the auxiliary materials, mixing, pelletizing, drying, granulating, and finally subpackaging. The enrofloxacin effervescent granule is developed according to veterinary drug GMP (Good Manufacturing Practice) standards by using modern detection means and pharmaceutical equipment, and is good in curative effect and is safe and reliable; the auxiliary materials and an effervescent disintegrating agent are added to the raw materials to prepare the effervescent granule; and the sick livestock administrates orally, the enrofloxacin effervescent granule is good in mouth feel and stable in quality, and the bioavailability of medicine is improved.
CN102440967A Rabeprazole sodium for injection as well as preparation method and detection method thereof The invention relates to rabeprazole sodium for injection as well as a preparation method and a detection method thereof. The rabeprazole sodium for injection is a medical preparation for injection, which is prepared from rabeprazole sodium as an active ingredient, a stabilizing agent, a pH value regulator and pharmaceutically acceptable auxiliary materials. The rabeprazole sodium for injection, disclosed by the invention, is rapid in effect taking and high in bioavailability, is used for treating gastrohelcosis, duodenal ulcer, erosive gastroesophageal reflux disease, helicobacter pylori injection, Zollinger-Ellision syndrome and the like and is more suitable for being used as a substitutive medicament when oral preparations for treating the diseases have no effect.
CN102247332A Lamivudine tablet and preparation method thereof The invention belongs to the field of pharmaceutical preparation, and especially discloses a lamivudine tablet and a preparation method thereof. The lamivudine tablet comprises lamivudine, lactose, low-substituted hydroxypropyl cellulose, cross linked sodium carboxymethyl cellulose, hydroxypropyl methylcellulose and magnesium stearate in a certain ratio. The invention has advantages of low costs, easy operation, stable and controllable product quality, and good dissolution rate; besides, relative quality indexes have certain advantages compared with those of products prepared by foreign companies.
CN101234124A Method of preparing crystallization physiotherapeutic salt The invention discloses a production method of a large granule physiotherapy salt, which comprises the working procedure of: slat slurry taking, crystal growing, washing, centrifugal separation, drying and screening, etc. Compared with the conventional refined salt, the crystal physiotherapy salt prepared via the method in the invention is characterized in large particle size, high purity and high quality, has good moisture-resistance ability and anti-caking ability; moreover, as the crystal physiotherapy salt is of small specific surface area, higher enthalpy, slow heat release and longer constant temperature time, which is more suitable for physiotherapy. At the same time, the method of the invention prepares the shape of the physiotherapy salt to be spherical granule, resulting in a structured shape, which is more favorable for improving the anti-caking ability and heat preservation ability, and more favorable for using in the mode of direct contact with human body.
US20080267867 Imidazole, pyridine derivative silver complexes; nanofiber with radioactive transition metal, lanthanide, actinide; radiopharmaceutical peptide, polyamine, imaging and tumor treatment A method for inhibiting microbial growth comprises administering an effective amount of a silver complex of a N-heterocyclic amine. A method for treating cancer cells or a method for imaging one or more tissues of a patient includes administering an effective amount of a complex of a N-heterocyclic amine and a radioactive metal. N-heterocyclic carbenes of the present invention may be represented by formula (I) wherein Z is a heterocyclic group, and R1 and R2 are, independently or in combination, hydrogen or a C1-C12 organic group selected from the group consisting of alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, arylalkyl, alkylaryl, heterocyclic, and alkoxy groups and substituted derivatives thereof.
WO2008118790A1 Dihydroindazole compounds useful in treating iron disorders This invention is directed to compounds of formula (I): wherein formula (A), m, R1, R2, R3 and R4 are are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.
WO2007053353A3 Pyrrolo[2,3-f] and [3,2-f]isoquinolinone derivatives as 5-hydroxytryptamine-6 ligands The present invention provides a compound of formula I or II and the use thereof in the therapeutic treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
EP2074085A2 Anti-infective thiourea compounds The present application discloses thiourea compounds for use in the treatment of infections. The thiourea compounds have formula (I) wherein X1 and X2 each designate one or more substituents; and Z is-(CHR)-, -(CHR)2-, -O-(CHR)2-, -NH-(CHR)2-, or -S-(CHR)2-; including salts thereof.
CN101411746A Novel use of salvia root extract The invention belongs to the field of pharmacology and discloses novel application of radix salviae miltiorrhizae extract. The radix salviae miltiorrhizae extract is used for preparing a composition for reducing myocardial vacuolation. The inventor accidentally finds out that the radix salviae miltiorrhizae extract has superior effect on reducing myocardial vacuolation and has no side effect. The radix salviae miltiorrhizae extract can be combined with adriamycin for use, and greatly reduce the toxic and side effect after application of the adriamycin, so that the radix salviae miltiorrhizae extract can inhibit tumor and simultaneously reduce myocardial vacuolation.
CN101584666A Preparing method of proton pump inhibitor biological adhesive preparation The invention discloses a preparing method of a proton pump inhibitor biological adhesive preparation, which comprises the following steps: selecting peroral proton pump inhibitor medicaments, alkaline substances, carrier materials and biological adhesive materials to prepare the adhesive preparation by a preparation preparing method; making enteric coating on the outer layer of the preparation; and finally, preparing the medical preparation containing the adhesive materials. The proton pump inhibitor biological adhesive preparation prepared by the preparing method has the advantages of indissolvableness in gastric acid, coating film degradation in intestinal juice, and the like, is adhered to the intestinal mucosa for slowly releasing, and is suitable for treating gastric ulcer and duodenal ulcer.
US8067466 Cycloalkyl-hydroxyl compounds and compositions for cholesterol management The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
CN1858068A Method for preparing pollen pini polyose, pollen pipe polyose and its use in medicine The process of preparing pollen pini polyose includes the following steps: 1. decocting wall broken pollen pini to extract and filtering; 2. enzymolyzing with pancreatin and cellulose, centrifuging at high speed and ultrafiltering to eliminate impurity; 3. alcohol precipitating the filter residue liquid, and drying the precipitate to obtain coarse pollen pini polyose; 4. eluting coarse pollen pini polyose in DEAE-cellulose column; and 5. nanofiltering, concentrating the filter residue liquid, drying and crushing to obtain single pollen pini polyose. The present invention also discloses the medicinal application in preparing medicine for lowering blood fat, blood pressure and blood sugar, resisting fatigue and raising immunity. The present invention provides one new way for developing and utilizing pollen pini.
EP1246640B1 Method and composition for treatment and/or prevention of antibiotic-resistant microorganism infections The present invention relates to a new composition, use and method to improve the cure of infections caused by antibiotic resistant microbial pathogens, in particular beta-lactam resistant microorganisms. Lactoferrin (LF) or Lactoferricin (LFC) can be administrated alone or in combination with antibiotic to affect growth, physiology and morphology of targeted microorganism. Lactoferrin increase susceptibility and can reverse resistance of microorganism to antibiotics.
CN1757409A Recipe of Wanshou capsule, and health-care function A medicine í‹long life capsuleíŒ for preventing cardiovascular and cerebrovascular diseases, cancer and diabetes, and preventing and treating more than 40 diseases, such as chronic hepatitis, senile cataract, rheumatoid diseases, arthritis, lupus erythematosus, etc is prepared from polyase selenate, VC, VE, calcium salt of amino acid, the organic Fe, Zn and Cr, beta-carotene, lycopene and extract of ganoderma.
US20050065117 Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin D derivatives and a bisphosphonate The present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof a combination of a 2-alkylidene-19-nor-vitamin D derivative and a bisphosphonate. Particularly, the present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof 2-methylene-19-nor-20(S)-1α, 25-dihydroxyvitamin D3and a bisphosphonate.
CA2724569A1 Compositions and methods to protect cells by blocking entry of pathogen proteins Pathogenic effector proteins which include one or more RxLR, dEER, Pexel or analogous motifs are blocked from entry into plant or animal cells by binding one or more of the motifs with a blocking compound which prevents binding of phosphoinositides or other polar lipids to the motifs which is a prerequisite for translocation of the pathogenic effector proteins into the plant or animal cell. The blocking compounds can take a variety of forms including synthetic peptides or the hydrophilic head-groups of phosphoinositides, phosphatidic acids, phospholipids, or sphingolipids. Suitable blocking compounds can be identified by assays demonstrating binding to RxLR, dEER, Pexel or analogous motifs. In addition, pathogenic effector proteins can be identified by analyzing whether they contain structural RxLR motifs using hidden markov modeling.
WO2012084804A1 NOVEL ANTIFUNGAL 5,6-DIHYDRO-4H-PYRROLO[1,2-a][1,4]- BENZODIAZEPINES AND 6H-PYRROLO[1,2-a][1,4]BENZODIAZEPINES SUBSTITUTED WITH BICYCLIC BENZENE DERIVATIVES The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo- [1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with bicyclic benzene derivatives of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
WO2009036996A3 Small molecule bradykinin b1 receptor antagonists Disclosed are compounds of formula (I) which are bradykinin B1 receptor (B1R) antagonists. These compounds are useful to treat diseases or relieve adverse symptoms associated with inflammation and pain. The invention encompasses novel compounds and acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases involving inflammation and pain.
EP2549995A2 Use of anatabine to treat inflammation and methods of synthesizing anatabine Pharmaceutical compositions comprising an isolated form of anatabine or a salt thereof can be used to treat disorders comprising an inflammatory component, including chronic, low-level inflammation. In another aspect, methods for the synthetic preparation of anatabine involve reacting benzophenoneimine with 3-aminomethyl pyridine to form benzylhydrylidene-pyridin-3-yl-methyl-amine. The benzylhydrylidene-pyridin-3-yl-methyl-amine is treated with a non-nucleophilic base and a dielectrophile, such as cis-1,4-dichloro-2-butene, followed by acidification, then basification, to provide anatabine.
WO2013163239A1 Synthesis of lactams Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC------OR---NH-LG, wherein OR is an organic moiety and LG is a leaving group, is reacted with an acid, such as an organic acid, in particular a strong acid, and a dehydrating agent, which may be one in the same such as a strong acid anhydride, such that the amount of acid added allows for the desired transformation to take place without the loss of the leaving group (LG) before the cyclization, and recovering the lactam.
CN102138934A Emulsifiable paste for treating scabies The invention discloses emulsifiable paste for treating scabies, which comprises the following components in percentage by weight: 55 to 75 percent of vaseline, 15 to 30 percent of sulphur powder, 2 to 6 percent of diphenhydramine hydrochloride, 3 to 6 percent of camphor alcohol liquid and 0.04 to 0.1 percent of furacilin powder, wherein the camphor alcohol liquid is prepared by dissolving 15 to 20 grams of camphor block in 85 to 130 millimeters of medical alcohol. The emulsifiable paste for treating the scabies has the quick treatment effect on the scabies, takes effect obviously on mild and moderate patients within 3 days, cures the patients for about one week, and can relieve the uneasiness or pain of the patients fundamentally, and the scabies can be treated completely, and is difficult to relapse basically. In addition, the emulsifiable paste of the formula has low cost and a wide application range, is readily available, and is suitable for extensive ordinary families.
WO2013012007A1 Anti-virus agent composition Provided is an anti-virus agent composition which has low levels of irritation and corrosivity and also has an excellent effect of inactivating viruses, particularly an excellent effect of inactivating non-enveloped viruses such as a norovirus. An anti-virus agent composition comprising the following components (A) and (B): (A) 0.05 to 0.5 vol% inclusive of at least one quaternary ammonium salt selected from a dialkyldimethylammonium salt and an alkylbenzyldimethylammonium salt; and (B) 0.5 to 2 vol% inclusive of benzyl alcohol.
US20120015896 Anti-Penicillin Resistant Pneumococci Agent and Novel 16-Membered Macrolide Derivative A novel compound that has antimicrobial activity against penicillin-resistant Streptococcus pneumoniae, and an anti-penicillin resistant pneumococci agent that includes the compound as an active ingredient are provided. Thus, an anti-penicillin resistant pneumococci agent is provided that includes as an active ingredient a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof, or hydrates thereof: wherein, in the formula (I), R represents any one of a halogen atom, an azido group, Ra-Wa-, Rb-Wb-, Rc-Wc-, and RdRd′N—.
WO2009010560A1 Pyrazole derivatives and use thereof as inhibitors of stearoyl-coa desaturase The present invention relates to compounds of formula (I) and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds of formula (I) for inhibiting stearoyl-CoA desaturase (SCD) activity.
US8734780 Methods for treating cardiac pacing conditions The method may include administering to a subject in need thereof an effective amount of an HCN polynucleotide. The HCN polynucleotide includes a nucleotide sequence encoding an HCN polypeptide having channel activity. The amino acid sequence of the HCN polypeptide and the amino acid sequence of a reference polypeptide have at least 80% identity, where the reference polypeptide begins with an amino acid selected from amino acids 92-214 and ends with an amino acid selected from amino acids 723-1188 of SEQ ID NO:8. An example of a reference polypeptide is amino acids 214-723 of SEQ ID NO:8. The HCN polynucleotide may be DNA or RNA.
EP2736908A1 Bicyclic pyrimidone compounds The present invention relates to novel bicyclic pyrimidone compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
CN102010375A Rosuvastatin calcium compound with stable crystal form The invention relates to a rosuvastatin calcium compound with a stable crystal form as shown in the formula (I) and a preparation method thereof. The preparation method is characterized by comprising the following steps: step 1, dissolving rosuvastatin calcium in a mixed solution of methanol, water and activated carbon, wherein the ratio of methanol to water is 1:1; step 2, heating and refluxing the solution prepared in step 1 for 60 minutes, and carrying out thermal filtration to remove the activated carbon; and step 3, cooling the solution prepared in step 2 for devitrification for 2 hours at the temperature of below -5 DEG C, and collecting the stable crystal form through the filtration.
WO2008155035A3 Oxazolidinones for the treatment and prophylaxis of sepsis The invention relates to the use of factor Xa inhibitors, in particular of oxazolidinones of formula (I), for the treatment and/or prophylaxis of sepsis, disseminated intravascular coagulation, septic shocks, septic organ dysfunction, septic organ failure and/or ARD and use thereof for production of a medicament for the treatment and/or prophylaxis of sepsis, disseminated intravascular coagulation, septic shocks, septic organ dysfunction, septic organ failure and/or ARD.
CA2467769A1 Methods and formulations for testosterone suppression Compositions comprising immunogenic GnRH multimer/leukotoxin chimeras in combination with aluminum-based adjuvants and Montanide.TM., are described. The compositions elicit anti-GnRH antibodies and are useful for suppressing testosterone levels, e.g., in males with prostate cancer.
WO2007137954A1 Aryl-4-ethynyl-isoxazole derivatives The present invention is concerned with aryl-4-ethynyl-isoxazole derivatives of formula (I) wherein R1 to R5 are as described in the specification, R5 representing an optionally substituted aryl or heteroaryl. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 receptor binding sites, being useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
CN101274900A 2-hydroxy halogeno-benzyl amino acid compound, preparation therefor and application thereof The invention discloses a 2-hydroxyl halogenated benzyl amino acid compound and a preparation method and application thereof. The preparation technology of the 2-hydroxyl halogenated benzyl amino acid compound designed by the invention is simple and can enhance the fat-soluble performance of the compound and promote the compound absorption of cells due to that the compound molecules contain the structure of amino acid. After the amino acid introduces drug molecules, the amino acid can often be released by hydrolysis in the body so as to relieve the toxicity of drugs to the cells to some degree. Therefore, the compound can be taken as fungicide, the precursor compound of the fungicide and biological preparation raw material, etc. to be used, is suitable for sterilization, anti-virus, deodorization and the removal of adjunct outside the skin and can be used as anti-virus, antiviral drug, sterilizing and disinfecting reagents as well as the sterilizing components of daily chemicals and sanitary finishing agents, etc.
WO2006044903A1 HYDRATE OF N-METHYL-N-(3-{3-[2-THIENYLCARBONYL]-PYRAZOL-[1,5-α]- PYRAMIDIN-7-YL}PHENYL)ACETAMIDE AND PROCESSES AND METHODS RELATED THERETO A novel hydrate form of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide ('Compound No. 1') and processes related to the use thereof in the synthesis of a polymorphic form of Compound No. 1.
WO2012074968A1 Methods of reducing risk of hepatobiliary dysfunction during rapid weight loss with metap-2 inhibitors The invention generally relates in part to methods of reducing hepatobiliary dysfunction and reducing risk of incident hepatobiliary dysfunction, comprising administering a MetAP2 inhibitor to patients in need thereof. The invention also relates in part to methods of effecting weight loss while reducing hepatic injury or risk thereof, comprising administering a MetAP2 inhibitor.
EP1987029B1 Enantiopure quinuclidinyloxy pyridazines and their use as nicotinic acetylcholine receptor ligands This invention relates to novel enantiopure azabicyclo pyridazinyloxy derivatives of formula (I), which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
CN100998595A Medicine composition containing cefateram cyclodextrin capsule and its preparing method A composite medicine with high solubility, stability and activity and low hemolytic irritation contains cefteram ester and the pharmacologically acceptable dextrin chosen from beta-cyclodextrin and its derivatives. Its preparing process is also disclosed.
CN101279047B Oral medicament for curing cervical vertebra disease The invention discloses an oral drug for treating cervical spondylosis. The bulk drugs in whole of the oral drug comprises the ingredients as follows based on part by weight: 30 parts of rhizome of drynaria, 11 parts of monkshood, 30 parts of turtleback, 15 parts of rhizome of large-headed atractylodes, 40 parts of radix astragali, 30 parts of rhizoma ligustici wallichii, 50 parts of tuber of elevated gastrodia, 25 parts of suberect spatholobus, 25 parts of pawpaw, 2 parts of nux vomica, 12 parts of root of herbaceous peony, 10 parts of coring dark plums and 20 parts of root of kudzu vine, the common difference of each ingredient is controlled within plus or minus 2 percent; effective components are extracted from the ingredients of rhizoma ligustici wallichii, the tuber of elevated gastrodia, the rhizome of large-headed atractylodes, the radix astragali, the root of herbaceous peony, the rhizome of drynaria, the root of kudzu vine, the monkshood, the coring dark plums, the pawpaw andthe suberect spatholobus as additive components; the ingredient of nux vomica takes ground powder as an additive component; the ingredient of turtleback takes the dry extract, which is prepared by decocting ground turtleback, removing dregs and taking liquid medicine for concentrating, as an additive component; all the additive components are mixed, dried and ground to prepare the combination medicine. The oral drug has relatively strong pertinence and relatively obvious curative effects.
CN103191214A Preparation for relieving or neutralizing effect of alcohol and protecting liver The invention discloses a preparation for relieving or neutralizing the effect of alcohol and protecting the liver. The preparation comprises, by weight, 35 to 55% of the root of kudzu vine, 12 to 28% of pilose asiabell root, 12 to 28% of hovenia dulcis thumb, and 8 to 25% of Chinese-date. The preparation for relieving or neutralizing the effect of alcohol and protecting the liver comprises an oleanolic acid as a functional factor. The preparation has good effects of preventing drunkenness, relieving or neutralizing effect of alcohol and protecting the liver, can fast reduce ethanol concentration of blood after drinking, and can reduce the damage produced by ethanol on liver cells.
EP1430025B1 Methods and compositions for treating or preventing bacterial infection The invention relates to compositions and methods for treating or preventing disease or disorders caused by or associated with certain bacterial infection, especially Escherichia coli (E. coli) or Helicobacter pylori (H. pylori) infection.
WO2010029352A1 Treatment of fibrotic eye disorders using an mmp2 inhibitor Inhibitors of matrix metalloproteinase 2 are used to treat or prevent a fϊbrotic disorder of the posterior capsule of the eye, for example posterior capsule opacification (PCO), or of a tissue or structure of the eye other than the lens or capsular bag.
US20080003250 Novel therapy for herpesvirus infection The present invention relates to an implantable drug delivery device comprising a polymeric or polymeric containing material in combination with a therapeutic compound effective for the treatment of a member of the herpesvirus family, wherein the therapeutic compound is in an amount that will effectively treat HSV-1, HSV 2 and/or VZV or reduce reactivation, and wherein the implantable drug delivery device is positioned at or near the site of latent infection or at the site of observed clinical symptoms. The therapeutic compound may include any active antiherpes agent including acyclovir, guanosine, valacyclovir or functionally active analogues.
US20060198790 Buccal, polar and non-polar spray containing ondansetron Buccal aerosol sprays or capsules using polar and non-polar solvents have now been developed which provide ondansetron for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, ondansetron, and optional flavoring agent; formulation II: aqueous polar solvent, ondansetron, optionally flavoring agent, and propellant; formulation III: non-polar solvent, ondansetron, and optional flavoring agent; formulation IV: non-polar solvent, ondansetron, optional flavoring agent, and propellant; formulation V: a mixture of a polar solvent and a non-polar solvent, ondansetron, and optional flavoring agent; formulation VI: a mixture of a polar solvent and a non-polar solvent, ondansetron, optional flavoring agent, and propellant.
EP1695701A2 HFA suspension formulations comprising an anticholinergic agent Suspensions of crystalline tiotropium bromide monohydrate (I) in the propellant gases HFA 227 and/or HFA 134a, optionally mixed with one or more further propellant gases selected from propane, butane, pentane, dimethyl ether, difluoromonochloromethane, difluoromethane, isobutane, isopentane and/or neopentane, are new. - ACTIVITY : Antiasthmatic; Antiinflammatory. - MECHANISM OF ACTION : Anticholinergic.
US20080009505 Theanine derivatives, uses thereof and processes for the manufacture thereof The present invention provides compounds, including peptides, which comprise theanine and/or theanine-like moieties. These compounds may deliver the physiological effects of theanine and/or offer enhanced storage stability. Also provided is a process for manufacturing the compounds by reacting theanine or a derivative thereof with at least one amino acid or a derivative thereof.
US7186849 C7 ester substituted taxanes Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
US7244711 Mixtures of enzyme inhibitors and free radical scavengers selected from phenolic compounds, phenothiazines and diphenylamines, used for prophylaxis of rheumatic diseases, pancreatitis, multiple sclerosis or gastrointestinal disorders The invention concerns a pharmaceutical composition comprising, as active principle, at least a calpain inhibiting substance and at least a substance trapping reactive oxygen species (ROS), and optionally an acceptable pharmaceutical carrier. The invention also concerns a product comprising at least a calpain inhibiting substance and at least a substance trapping reactive oxygen species (ROS), selectively or not, as combination product, the active principle being separate.
CN102935169A Externally-applied drug for promoting quick healing of wound The invention relates to an externally-applied drug for promoting quick healing of wound, containing the following components: 5-10g of borneol, 100-150g of gypsum, 20-30g of bulbus fritillariae cirrhosae, 4-8g of common monkshood mother root, 10-30g of pinellia ternate, and 10-15g of dragon blood. The components are smashed, stirred and mixed to be uniform, so as to prepare the externally-applied drug. The externally-applied drug can effectively realize sterilization and detumescence, and simultaneously can promote tissue regeneration, integrates two efficacies, and is short in treatment period, quick in effect and also suitable for persons with sensitive skin.
CN1850105A Pharmaceutical use of glycoconjugates CHB for preventing and treating avian flu The present invention discloses an application of saccharic conjugate CHB in preparation of medicine for preventing and curing epidemic influenza or fowl influenza. The tests show that the saccharic conjugate CHB has the effect of raising immunity of body.
US20080051440 Compositions for weight management Methods and compositions for regulating food intake in a human subject; for improving a compliance of a human subject to caloric restriction; and for reducing a desire of a human subject to consume fats, utilizing H1-receptor agonists that have a pharmacological half-life that allows am efficient treatment regime thereof are disclosed. The methods and compositions can be efficiently used for treating conditions such as overeating, overweight, obesity, binge eating disorder, night eating syndrome, obsessive eating, compulsive eating and bulimia, as well as conditions associated with metabolic derangement such as dyslipidemia and for preventing or reducing weight gain due to factors such as drug use, cessation of smoking, and the like in a human subject.
CN101837018A American cockroach medicinal composition for curing ulcers or ulcerative inflammation and preparation method thereof The invention discloses an American cockroach medicinal composition for curing ulcers or ulcerative inflammation. The medicinal composition is mainly prepared from an active ingredient mixture prepared by mixing an American cockroach extract and montmorillonite powder. The weight part ratio of the American cockroach extract to the montmorillonite powder is equal to 0.8-1.2:0.5-6. A preparation method of the American cockroach medicinal composition for curing the ulcers or the ulcerative inflammation comprises the following steps of: preparing the American cockroach extract, mixing active ingredients, and preparing medicaments. The medicinal composition has simple preparation method, fully exerts effects of the American cockroach extract, and has obvious effects of effectively curing diseases such as oral ulcers, recurrent aphthous ulcers, oral lichen planus, oral mucosal injury (behcet disease, herpes simplex, leukoplakia, discoid lupus erythematosus, hand-foot-and-mouth disease, scalds, chemotherapy, radiotherapy and the like) caused by various reasons, reflux esophagitis, eophageal ucers, radiation esophagitis, ulcerative colitis, radiation proctitis, and diarrhea, and hematochezia with mucosal injury, and the like.
WO2008066032A1 Lymphangiogenesis inhibitory factor Disclosed are: a lymphangiogenesis inhibitor comprising vasohibin; a lymphangiogenesis inhibitor comprising a vector carrying a polynucleotide encoding vasohibin; a pharmaceutical composition for the treatment of a disease for which a lymphangiogenesis inhibitory effect is required, which comprises the inhibitor; use of vasohibin for the production of a pharmaceutical composition for the treatment of a disease for which a lymphangiogenesis inhibitory effect is required; use of a polynucleotide encoding vasohibin for the production of a pharmaceutical composition for the treatment of a disease for which a lymphangiogenesis inhibitory effect is required; and a method for the treatment of a disease for which a lymphangiogenesis inhibitory effect is required, which comprises the step of administering the inhibitor. The inhibitor can be used suitably for the treatment of a disease for which a lymphangiogenesis inhibitory effect is required or the like.
US20120213737 Compositions and methods for therapeutic membrane repair Disclosed herein are compositions comprising PTRF polypeptides, nucleic acids, and PTRF binding proteins useful for tissue regeneration and the treatment and prevention of disorders relating to cell membrane damage and repair.
CN1883474A A composition containing macrolide compound and porous water insoluble hydrophilic carrier The invention discloses a composition comprising macrolide compounds and porous water-insoluble hydrophilic carrier. By using one or more porous water-insoluble hydrophilic carriers to replace water-soluble carriers, the objective of increasing dissolving rate and improving biological availability can be achieved.
CN101219104A Cladribine sustained-release implantation agent for treating solid tumors The invention relates to a sustained-release implant for treating solid tumors, which is characterized in that the sustained-release implant contains Cladribine and sustained-release excipient of effective anticancer amount. The solid tumors comprise brain tumor, liver cancer, lung cancer, esophageal cancer, carcinoma ventriculi, mammary cancer, pancreatic cancer, cancerous goiter, nasopharyngeal darcinoma, oophoroma, endometrial carcinoma, carcinoma of uterine cervix, renal carcinoma, prostatic carcinoma, carcinoma of urinary bladder, carcinoma of colon, rectal cancer, cutaneum carcinoma, head and neck cancer and primary or secondary cancer, caruncle or carcinosarcoma from peripheral nervous system, mucosa, body of gland, blood vessel, bone tissue and absorbent gland. The sustained-release excipient is mainly degradable high molecular polymer with biological capacitability, and carmustine is slowly released into local tumor during the degradation and absorption process, therefore the invention not only obviously reduces the toxic reaction to the whole body, but also maintains effective drug concentration at the local tumor. The sustained-release implant is arranged in the local tumor, which not only reduces the carmustine toxic reaction to the whole body, but also increases the drug concentration at the local tumor selectively, thereby improving treatment effect of chemotherapeutics, radiotherapeutics and other non-operative treatment.
WO2014142550A1 Phenyl carbamate compound and a composition for preventing or treating a psychiatric disorder comprising the same The present invention relates to a composition for preventing or treating a psychiatric disorder comprising a phenyl carbamate compound and a method for preventing or treating a psychiatric disorder therewith. The present invention provides anti-anxiety activity and protections against seizure and bipolar disorder, such that it may be effectively used for preventing or treating various psychiatric disorders related to mood disorder or resulting convulsion.
US20110003757 Pharmaceutical compositions for treating fatty liver disease The present invention provides a pharmaceutical composition useful as a therapeutic agent for fatty liver disease. A pharmaceutical composition, which comprises (1S)-1,5-anhydro-1-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, (1S)-1,5-anhydro-1-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, or alternatively, (1S)-1,5-anhydro-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, more specifically such a pharmaceutical composition for treating fatty liver disease, such as nonalcoholic fatty liver disease in one embodiment, or nonalcoholic simple fatty liver and/or nonalcoholic steatohepatitis in another embodiment.
CN101341137A Pyrazine derivatives as epithelial sodium channel blocker A compound of formula (I) or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, T, L, W, X, Y and A are as defined herein, for the treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergic condition.
US20100215728 Skincare Methods Disclosed are compositions and methods for skincare, e.g., reducing skin wrinkles and for treating skin disorders.
WO2010024225A1 Novel dihydrotriazine derivative A compound represented by general formula (1), a tautomer thereof, or a salt of the compound or tautomer, which is useful as a bactericide/disinfectant. (In the formula, R1 represents a hydrogen atom, an optionally substituted alkyl group or the like, R2 represents a hydrogen atom or an optionally substituted alkyl group, or alternatively R1 and R2 may combine together with an adjacent nitrogen atom to form an optionally substituted nitrogen-containing heterocyclic group; R4 represents a hydrogen atom or an optionally substituted alkyl group; R3 represents an optionally substituted alkyl group; and R5 and R6 each represents a hydrogen atom or a methyl group. In this connection, a compound wherein both R2 and R4 represent a hydrogen atom and a compound wherein both R1 and R4 represent a hydrogen atom are excluded.)
US20090239820 Compounds and methods for treatment of solid tumors The present invention relates to pharmaceutical compositions containing targetable bioconjugates of hydralazine, a direct vasodilating agent previously shown to decrease tumor blood flow, oxygenation and interstitial fluid pressure in solid tumors. These bioconjugates are hydralazine prodrugs that contain hydralazine conjugated to biocompatible carrier molecules which specifically bind to sites that are expressed on a diverse variety of tumor cell types. These hydralazine prodrugs are preferably conjugated through an acid-labile hydrazone link that is designed to be stable in plasma and release hydralazine through acid-catalyzed hydrolysis in the acidic environment of the target tumor. Because these prodrugs are stable at physiological pH and in plasma, they are devoid of systemic vasoactive activity; however, they are acid-labile conjugates that can be hydrolyzed upon reaching the more acid environment of the tumor where the vasoactive activity of hydralazine is restored. These prodrugs selectively bind to tumor-specific receptors on tumor cells, and are degraded in the acidic tumor cell environment or the acidic lysosomal compartments after being internalized into the cell.
CN103405432A Medicinal combination containing ilaprazole sodium and naproxen The invention provides a medicinal combination containing ilaprazole sodium and naproxen. The medicinal combination is formed by using the ilaprazole sodium and the naproxen as active ingredients and mixing the ilaprazole sodium and the naproxen with pharmaceutically-acceptable auxiliary materials. In the medicinal composition, the weight ratio of the ilaprazole sodium to the naproxen is (1:10)-(1:30), preferably 1:16. The medicinal combination can be made into an oral preparation and used for curing patients with rheumatoid arthritis, ostarthritis and ankylosing spondylitis, wherein when the rheumatoid arthritis, the ostarthritis and the ankylosing spondylitis are treated with non-steroid anti-inflammatory drugs, the risks of gastric ulcer relapse can be caused.
US20100267722 Novel proline derivatives The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
CN101116664B Application of compound 1-( 4-chloroaniline )-4-( 4-picoline )-2, 3-naphthyridine The invention relates to the use of compound 1-(4-chlorobenzene amidocyanogen)-4-(4-methylpyridine)-2, 3-phthalazine in preparing medicine used for preventing tumor diseases, wherein the medicine contains 1-(4-chlorobenzene amidocyanogen)-4-(4-methylpyridine)-2, 3-phthalazine and is used through administration method via or outside intestines and stomach. The compound can at least prolong or avoidoccurrence or formation of tumor; moreover, tumor patient adopting medicine containing the compound for prevention obtains higher survival rate as compared with the patient who does not adopt the prevention method.
CN101053560A Taurine and anti-infectious medicine composition The invention belonging to medical technology field discloses a medicine combination containing mainly a 2-aminoethanesulfonic acid and at least an anti-infection medicine and its producing method and application, in which the anti-infection medicine is chosen from: one or more new houttuyfonate or the pharmaceutical acceptable salt, drographolide succinate and matrine. The medicine combination can be produced to different pharmacological acceptable formulation. The inventive medicine combination is mainly used for antipyretic-analgesic, anti-inflammatory function. The Pharmacological tests indicates the curative effect of the combination is better than the signal effect by only applying the 2-aminoethanesulfonic acid, houttuyfonate or the pharmacological acceptable salt, drographolide succinate and matrine with a same dose. The invention has a broad application prospect.
CA2373433C Spiroimidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them The present invention relates to spiroimidazolidine derivatives of formula (I) in which E, V, W, X, R1 and R2 have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmaceutical active compounds which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of formula (I) are inhibitors of the adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy and prophylaxis of illnesses which are caused by an undesired extent of leukocyte adhesion and/or leukocyte migration or are associated therewith or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part. The invention furthermore relates to processes for the preparation of the compounds of formula (I), their use and pharmaceutical preparations which contain compounds of formula (I).
US20110301173 1-heterocyclylsulfonyl, 3-aminomethyl, 5- (hetero-) aryl substituted 1-h-pyrrole derivatives as acid secretion inhibitors The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
EP0951295B1 Compositions for use in inhibiting of alpha-v-beta3 mediated angiogenesis The present invention describes methods for inhibition of angiogenesis in tissues using vitronectin αvβ3 antagonists, and particularly for inhibiting angiogenesis in inflamed tissues and in tumor tissues and metastases using therapeutic compositions containing αvβ3 antagonists.
EP2652136A1 Nucleic acids targeting tctp for use in the treatment of chemo-or hormone-resistant cancers The present invention concerns a TCTP antagonist, in particular a nucleic acid targeting an m RNA encoding Translationally-Controlled Tumor Protein (TCTP), wherein said nucleic acid is capable of reducing the amount of TCTP in cells, for use in the treatment or prevention of hormone-independent cancer or chemo-resistant cancer, such as an androgen-independent prostate cancer.
US20110207741 Activation of the Renin-Angiotensin System (RAS) and Sudden Cardiac Death Provided herein are methods of treating a medical condition in which RAS activation is increased. The method comprises the step of administering to a subject a c-Src inhibitor in an amount effective to treat the medical condition. The invention also provides a method of treating or preventing a cardiac arrhythmia. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to treat or prevent the cardiac arrhythmia. The invention additionally provides a method of delaying the onset of sudden cardiac death. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to delay the onset of SCD. Methods of augmenting gap junction function and methods of increasing Connexin 43 levels in a subject in need thereof are further provided.
CA2553115A1 Modulation of peroxisome proliferation-activated receptors A method of treating a peroxisome proliferators-activated receptors related disease by administering to a subject in need thereof an effective amount of a modulator of 15-keto prostaglandin-.DELTA.13-reductase. Also disclosed are methods of identifying a compound for inhibiting activity of the reductase and of lowering blood glucose levels by administering to a subject an effective amount of a reductase inhibitor.
US20130034530 Dietary Supplement Cognitive Support System The present invention relates to a nutritional supplement composition, comprising a therapeutically effective amounts of Vitamin C, Vitamin D3, Thiamin, Riboflavin, Niacin, Vitamin B6, Folic acid, Vitamin B12, Pantothenic acid, Calcium, Magnesium, Zinc, Chromium, Sugar, Protein, Acetyl-L-Carnitine, Dimethylaminoethanol complex, Phosphatidylserine complex, L-Glutamine, N-Acetyl-L-Tyrosine, L-Phenylalanine, Taurine, Methionine, Valine, Isoleucine, 5 Hydroxytryptophan, L-Taurine, N-Acetyl-Tyrosine, N-Acetyl-L-Cysteine, Alpha Lipoic Acid, Alpha Glycerylphosphoricholine complex, Bacopa Monnieri extract, Gingko Biloba extract, Passion flower, Lemon Balm, Gotu Kola, Ashwagandha, Choline Bitartrate complex, Panax Ginseng extract, Turmeric, Organic freeze dried fruit juice blends (concord grape, red raspberry, pineapple, cranberry, acai, pomegranate, acerola cherry, bilberry, lingonberry, black currant, aronia, sour cherry, black raspberry), Organic freeze dried greens blends (barley grass, broccoli, beet, carrot, alfalfa, oat), and Protein digestive enzyme blends (Protease 4.5, peptidase, bromelain, protease 6.0, protease 3.0, L planatrum, B bifidum) in a mixture to provide optimal cognitive function.
CN101574328B Timing pulsed release micro-pill of zolpidem salt The invention relates to the field of pharmaceutical preparations, in particular to a timing pulsed release micro-pill of a zolpidem salt, which is characterized in that the center of the micro-pill is a blank pill core, an external time-lag layer is coated by low-permeability acrylic resin containing quaternary ammonium salt radicals, and a medicament layer and an organic acid layer are arrangedbetween the blank pill core and the time-lag layer, wherein the organic acid layer contains a mixture of two organic acids, and the mixture of the two organic acids is prepared by mixing one of succinic acid, glutaric acid and adipic acid, and one of citric acid, malic acid and tartaric acid. Combining with sleep characteristics of early awakening crowds, the prepared micro-pill has certain release time lag and releases quickly after a period of time lag so that a patient obtains effective blood concentration on the point of awakening so as to prolong the sleep time of the patient.
WO2013023102A1 Inhibiting transient receptor potential ion channel trpa1 This disclosure describes a novel compounds and pharmaceutical compositions for inhibiting the TRPAl ion channel and/or medical conditions related to TRPAl, such as pain or asthma.
EP2350080A1 Unsymmetrical pyrrolobenzodiazepine-dimers for treatment of proliferative diseases Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables R12 and R2 represent. Formula (I), wherein: R2 is of formula (II), where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N=C=O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and -Z-(CH2)n-, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is -CH=CH-, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases.
EP1646381A2 Combination therapy for treating chronic inflammatory diseases The present inventions is directed to a novel DMARD sparing method for treating chronic inflammatory diseases or conditions, such as rheumatoid arthritis, comprising the short-term administration of a disease modifying anti-rheumatic drug (DMARD) followed by reduction of the DMARD and co-administration of a cyclooxygenase-2 selective inhibitor or cessation of the DMARD and continued maintenance therapy using a COX-2 selective inhibitor alone. The present invention provides for an effective DMARD sparing therapy in patients suffering from inflammatory diseases or conditions.
WO2013057711A1 Quinazoline derivatives as pi3k modulators The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X1, X2, X3, X4 and R5 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
CN101555245A Application of silibinin methyl ether in preparing anti-leukemia medicine The invention relates to the applications of silibinin methyl ether in preparing anti-leukemia medicine, in particular to a novel preparation method of silibinin derivative 7, 20-dimethyl silibinin, and the applications of the compound or the medicinal salt thereof in preparing medicines for preventing and treating lymphatic leukemia and medullocell leukemia, and the compound is prepared by the single-step reaction of a natural drug-the silibinin. Proved by pharmacological test: the compound has strongly effective inhibiting effect to the in-vitro proliferation of both transplantable mouse lymphatic leukemia P388 cell and human acute medullocell (promyelocytic) leukemia cell strain HL-60 cell, and the IC50 values thereof are respectively 7.1 plus or minus 1.8 micromol/L and 5.5 plus or minus 1.9 micromol/L.
WO2010108417A1 Method for preparing acyclovir 2/3 hydrate Preparation of acyclovir 2/3 hydrate comprises adding acyclovir into water at weight ratio of 1:5-50, dissolving at 50-100℃, filtering, cooling filtrate at 0-30℃ to separate crystal, filtering filtrate, collecting crystal, and drying crystal at 0-150℃ for 0.5-24 hours to obtain acyclovir 2/3 hydrate. The preparation process is simple and suitable for industrial production. The prepared product has good and stable crystal form.
EP1373194B1 BENZAMIDE INHIBITORS OF FACTOR Xa Novel benzamide compounds of formula (I), their salts and compositions related thereto having activity against mammalian Factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders wherein: Ar1, Ar2 and Ar3 are each independently selected from the group consisting of formula (II).
US6989386 Pharmaceutically active ornithine derivatives, ammonium salts thereof and methods of making same In one embodiment, the present invention relates to a new class of ammonium salts of Nδ-acyl derivatives of Nα-(4-amino-4-deoxypteroyl)-L-ornithine compounds having a structure according to formula II-IV. Formula II has the structure of: wherein: R2 represents up to four groups independently selected at each occurrence of R2 from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C1-6 alkoxy, chloro, fluoro, hydroxy, and —COOH; R3, R4, and R5 are each independently selected from hydrogen and C1-6 alkyl; or NR3R4 taken combination can form a 5 to 7 member heterocycle having at least one nitrogen ring atom; and x is a real number greater than 0 and less than about 4. The ammonium salts provided by the invention exhibit high inhibitory activity against the growth o methotrexate-resistant cells, and also exhibit superior chemical stability than corresponding acidic Nδ-acyl derivatives of Nδ-acyl derivatives of Nα(4-amino-4-deoxypteroyl)-L-ornithine compounds.
WO2007026251A3 Use of dual c-kit/fgfr3 inhibitors for treating multiple myeloma The present invention relates to a method for treating Multiple Myeloma (MM), FGFR3+ myeloma, especially relapsed or refractory multiple myeloma (4/14) expressing FGFR3, comprising administering a dual C-KIT / FGFR3 inhibitor, such as 2-aminoarylthiazoles and 2-aminoaryloxazoles.
US20130005814 Methods and compositions for facilitating weight loss by administration of thyroid hormones The present invention provides methods and compositions for facilitating weight loss in subjects who are undergoing a weight loss regimen by administration of thyroid hormones, for example, T2 alone, T2 in combination with T3, T2 in combination with T3 and T4, or T3 in combination with T4. In particular, subjects who have already experienced weight loss often are unable to continue to lose weight as the body experiences a famine response, i.e., hypothyroidism. By administration of the compositions of the present invention, for example, T2 alone, T2 in combination with T3, T2 in combination with T3 and T4, or T3 in combination with T4, subjects are able to return thyroid levels to normal and/or to reduce the levels of rT3 to normal, so as to allow the body to continue to lose weight.
CA2431984C Antibiotic coating for porous bodies and method for its production as well as its use The invention describes an antibiotic coating for porous bodies and its use. Into the porous system of non-metallic porous bodies and of metallic porous bodies, a coating made of at least one antibiotic salt that is hardly soluble in water or in an aqueous environment from the group of the netilmicin laurate, the netilmicin myristate, the netilmicin dodecyl sulfate, the sisomicin laurate, the sisomicin myristate, the sisomicin dodecyl sulfate, the gentamicin laurate, the gentamicin myristate, the clindamycin laurate, the amikacin laurate, the amikacin myristate, the amikacin dodecyl sulfate, the kanamycin laurate, the kanamycin myristate, the kanamycin dodecyl sulfate, the tobramycin laurate, the tobramycin myristate, the tobramycin dodecyl sulfate, the ciprofloxacin myristate, the vancomycin dodecyl sulfate, the vancomycin laurate, the vancomycin myristate, the vancomycin teicoplanin and the clindamycin teicoplanin is introduced. The antibiotically coated, porous bodies are used as implants.
CN1600857A RIP5 gene and usage This invention relates to RIP5 gene and its usage. In this invention, sequence homology alignment is used to obtain a novel gene RIP5. The experimental results shows that: said gene and its coded protein can induce cell to death. So, in the selection of medicine for treating and preventing cancer and the like diseases relating cell death medicine, it can be used for molecular target marking or diagnostic labelling.
US20130058980 Small molecule inhibitors of protein kinases Compounds that modulate, for example, that inhibit, syk kinase, and, optionally other kinases. The compounds can be used to treat a variety of disorders, including inflammatory disorders and autoimmune disorders.
CN101978951A 9,10-diphenylanthracene(DPA) ester fat emulsion intravenous injection and manufacturing method thereof The invention provides a DPA ester fat emulsion intravenous injection and a manufacturing method thereof. The manufacturing method comprises: mixing raw materials including DPA (dcosapentenoic acid) ester, lecithin, glycerol, sterile pure water, antioxygen, stabilizer, pH regulator and the like in the presence of protective nitrogen, stirring forcefully and shearing at high speed to obtain initial emulsion; emulsifying by using a high-pressure homogenizer and filtering by using a microporous membrane filter; and filling, sealing, and sterilizing to obtain the DPA ester fat emulsion intravenous injection. The DPA ester may be DPA methyl ester, DPA ethyl ester, DPA ethyl diester, DPA propyl diester and DPA triglyceride, and the DPA content of the DPA ester is over 90 percent. The DPA ester fat emulsion intravenous injection can be used in the field of medical care and heath and can be administrated through parenteral intravenous injection, enteral tube feeding or oral taking and serve as a nutritional and therapeutic medicament.
US20110136833 Tetrahydropyridinyl and Dihydropyrrolyl Compounds and the Use Thereof The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X, Y, Z, R1, R2, m, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
US20080183003 Neuroprotective agents; nitrate-functional, for example 1-amino-3,5-dimethyl-7-nitrateadamantane hydrochloride The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions. There are a variety of neurological disorders that can be treated using the present invention, including, for example, the following: neurological disorders arising from trauma, ischemic or hypoxic conditions that can be treated include stroke, hypoglycemia, cerebral ischemia, cardiac arrest, spinal cord trauma, head trauma, perinatal hypoxia, cardiac arrest and hypoglycemic neuronal damage; neurodegenerative disorders such as epilepsy, Alzheimer's disease, Huntington's disease Parkinsonism, and amyotrophic lateral sclerosis; other diseases or disorders such as convulsion, pain, depression, anxiety, schizophrenia, muscle spasms, migraine headaches, urinary incontinence, nicotine withdrawal, opiate tolerance and withdrawal, emesis, brain edema, tardive dyskinesia, AIDS-induced dementia, ocular damage, retinopathy, cognitive disorders, and neuronal injury associated with HIV-infection such as dysfunction in cognition, movement and sensation.
CN1568960A High purity chlorogenic acid prescription The invention relates to the medicament by using high purity chlorogenic acid as raw material, wherein the chlorogenic acid content is 95%-105%, the medicament can be prepared into different dosage forms including injection, germ-free powder injection, tablet, capsule, oral liquid, eye drops, ointment, and various controlled release formulation.
CN101028041B Slow-settling swelling ranular complex feed for large-yellow croaker scrod A slow-depositing composite puffed particle feed for the minnow of large yellow croaker is proportionally prepared from fish powder, wheat flour, bean dregs, refined corn protein, fish oil, beer yeast, shrimp shell, minerals, choline chloride, and vitamins.
CN103272204A Foot soaking powder for dysmenorrhea and stomach warming tea accompanied for drinking The invention discloses a foot soaking powder for dysmenorrhea and a stomach warming tea accompanied for drinking. The foot soaking powder comprises the following components: 3.8-4kg of motherwort, 2.2-2.4kg of dried ginger, 0.2-0.3kg of jujube leaves, 1.1-1.2kg of folium artemisiae argyi, and 1.5-1.6kg of salt. The stomach warming tea comprises the following components: 4.5-5kg of the motherwort, 2-2.2kg of peach kernel, and 3.8-4kg of brown sugar. The foot soaking powder for the dysmenorrhea and the stomach warming tea accompanied for drinking are prepared from a plurality of purely herbaceous plants. When a woman suffers the dysmenorrhea, the foot soaking powder can be used for foot soaking and washing, at the same time the stomach warming tea can be accompanied for drinking, and the stomach warming tea can warm stomach and dispel cold, dissipate stasis and expel toxin, and alleviate the dysmenorrhea.
CN103070856A Composition containing andrographolidi natrii bisulfis and preparation method and application thereof The invention relates to a composition containing andrographolidi natrii bisulfis and a preparation method and application thereof. The composition further comprises methionine and ethylene diamine tetraacetic acid salt, the content of the methionine is by weight 0.1% to 2% of the sodium andrographolide hydrogen sulfite, the content of the ethylene diamine tetraacetic acid salt is by weight 0.1% to 2% of the sodium andrographolide hydrogen sulfite, and the pH ranges from 4.0 to 4.8. When the composition containing sodium andrographolide hydrogen sulfite is used as an injection solution, the composite can tolerate excessive sterilization when the temperature is 121 DEG C and the F0>=12, and further the sterile level of the injection solution is further improved. In addition, the composition shows good stability when acceleration tests and long-term tests are performed according to national stability research technique guiding principles.
US7666906 β-Benzyloxyaspartate derivatives with amino group on benzene ring L-threo-β-benzyloxyaspartate derivatives having a substituent on the benzene ring, represented by the following formula (1): wherein R is hydrogen, a linear or branched lower aliphatic acyl group with the acyl portion optionally substituted, an alicyclic acyl group, an aromatic acyl group with a substituent on the aromatic ring, an amino acid-derived group or a biotin derivative-derived group, having an amino substituent on the benzene ring, and salts thereof, which can easily bind to affinity column chromatography carriers as ligands of glutamate transporter proteins.
CN101756991B Sustained-release pills of alfuzosin hydrochloride The invention belongs to the field of western medicine preparation, and more particularly relates to alfuzosin hydrochloride sustained-release pill preparation which mainly comprises medicine, pill matrix and sustained-release material. A dropping method for preparing the pills has simple equipment, convenient operation, short production cycle and accurate dosage; in the operation process, the medicine loss is low, the quality is stable, and the medicine is released at the speed approaching to zero-order release. Furthermore, the blood concentration in the human body is maintained to be stable, the medicine treating time in the human body is moderate, the side effect is lower, and drug resistance is not easily caused after the medicine is taken for a plurality of times.
CN101744958A Powdered medicine for treating epilepsy The invention relates to a powdered medicine for treating epilepsy. The powdered medicine for treating epilepsy is made from scorpion, ginger, cow bezoar, scolopendrid, Rheum pumilum, Potassium alum, Chinese white olive and batryticated silkworm as raw materials. Practices indicate the powered medicine for treating epilepsy has effectiveness of expelling endogenous wind to relieve convulsion, counteracting toxic substances and dissipating stagnation against the epilepsy and can heal the convulsions/fits to return the body of a patient to normal as soon as possible.
EP1404675B1 Dpp-iv-inhibiting purine derivatives for the treatment of diabetes The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. (I)
US20050239813 Pharmaceutical compositions comprising fk506 derivatives and their use for the treatment of allergic diseases The invention provides ophthalmic compositions and methods treating the symptoms of ocular allergies. The principle active ingredient in these compositions and methods is macrolide compound, such as tacrolimus, ascomycin and rapamycin and their derivatives. Optimal concentrations and dosing regimens are provided.
WO2007113540A8 Regulating fat and carbohydrate oxidation in muscle tissue comprising controlling carnitine content in muscle Methods, compositions and substances for regulating fat and carbohydrate oxidation in the muscle tissue of human and/or animal bodies, which involve controlling the carnitine content of the muscle tissue. Regulating carbohydrate and fat oxidation, and particularly increasing the level of fat oxidation in accordance with the present invention, by providing substances compositions and methodologies in accordance with the present invention, enable medicaments to be manufactured and methodologies employed that find use in the treatment of disorders and conditions of the human and/or animal body caused by impairment of the usual level of fat oxidation, including obesity and type 2 diabetes.
WO2012059442A2 Neurotrypsin inhibitors The invention relates to acylamino-phthalic acid amides and related compounds of formula (I) wherein A is -CONR3R4, -NR5COR6, -NHR7, -OR8, -SR9, -CH2NR10R11, -(CH2)2-R12, -CH=CH-R12, -C≡C-R12, optionally substituted phenyl, optionally substituted thiophenyl, or optionally substituted 1,2,3-triazol-4-yl, W is hydrogen, hydroxy or carboxymethoxy, Y is carboxy, methoxycarbonyl or 2H-tetrazol-5-yl, and the various substituents R have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.
US20110135642 Pharmaceutical Compositions Comprising Antibodies Binding To EBV (Ebstein-Barr Virus) Protein BARF1 The invention relates to pharmaceutical and vaccine compositions comprising an antibody binding specifically to selected peptides of EBV protein BARF1.
CN1616430A Rosinyl acridine its producing method and use thereof The present invention relates to a kind of rosinyl acridine compounds and their production process and use. There are four rosinyl acridine compounds. These rosinyl acridine compounds are produced with dehydrogenated rosin as material and through constituting acridine cycle on the carbon cycle and synthesizing acridone, so that the synthetic rosinyl acridine compounds have bright color, high covering and high colorizing capacity, and other features. In addition, they exhibit excellent antiseptic activity, and may be used as additive, paint, medicine, etc.
WO2010028254A3 Substituted quinazoline inhibitors of growth factor receptor tyrosine kinases The present invention relates to new substituted quinazoline inhibitors of vascular endothelial growth factor receptor tyrosine kinase, epidermal growth factor receptor tyrosine kinase, and/or rearranged during transfection tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.
CA1341603C Acidic polysaccharide esters and process for their preparation Processes are provided herein for the preparation of acidic polysaccharide esters. One process comprises treating a quaternary ammonium salt of the polysaccharide with an esterifying agent, preferably in an aprotic solvent, and, if desired, salifying free carboxy groups in the partial esters obtained, or releasing salified groups in them.
CN1961889B Application of isoliquiritigenin in preparation of medicament for preventing and/or treating depression The invention discloses the novel use of isoliquiritin in the preparation of medicament for preventing and/or treating depression, wherein the medicament can be made into various clinically acceptable dose forms including capsules, tablets, pills, granules, turbid liquors, drop pills, oral liquid preparations, injections, aerosols, suppositories or subcutaneous administration forms.
WO2009127321A1 Benzofurane, benzothiophene, benzothiazol derivatives as fxr modulators The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).
CN101292991A Compound gelling agent containing clindamycinum The invention relates to compound gel containing clindamycin. The compound gels comprise effective dose of the clindamycin or medicinal salt or ester, Tretinoin and gel matrix. The invention is characterized in that the gel matrix is celluloses derivative, a preparation method as well as the detection and analysis methods of the gel are also related. The gel of the invention has the advantages of easy quality control, simple preparation technique and being suitable for industrial production.
CN101693731A Method for extracting purified plantarenaloside from herba lysimachiae, product of plantarenaloside and application of method The invention discloses a method for extracting purified plantarenaloside from herba lysimachiae, a product of plantarenaloside and application of the method. The method comprises the steps of extracting and filtering dried or fresh entire plants, overground parts or underground parts of herba lysimachiae by conventional technologies, concentrating the filter liquor into extractum through reducing pressure, adding macroporous resin into the extractum, using ethylalcohol to elute, collecting alcohol eluant, recovering the solvent to get crude plantarenaloside, repetitively implementing silica gel column chromatography, reversed phase chromatography or gel column chromatography for the crude plantarenaloside, and recovering and drying the solvent to get the purified plantarenaloside. The purified plantarenaloside prepared by the method has the advantages of high degree of purity and strong pharmacological activity, can be used as chemical standard product or reference product of herba lysimachiae or the extract of the herba lysimachiae in medicine detecting, and can be used as medicine material for preparation. The invention has the advantages of low cost, and is applied to large-scale production.
WO2008131501A3 New anti-viral nucleoside analogs The present invention relates to a series of novel nucleoside analogs which have been shown to possess antiviral activity, in particular against viruses of the family of the Picornaviridae. The invention therefore relates to the new nucleoside analogs, methods for their preparation, pharmaceutical compositions comprising them and to the nucleoside analogs for use as a medicament, more in particular antiviral medicament.
CN102085372A Application of Notch pathway inhibitor in treatment of tumors caused by activation of mTOR The invention relates to application of a Notch pathway inhibitor in treatment of tumors caused by activation of a mammalian target of rapamycin (mTOR) and an upstream pathway thereof, particularly relates to application of a Notch pathway inhibitor in preparation of a medicament for treating tumors of mammals comprising human beings due to activation of an mTOR and an upstream pathway thereof, and also relates to application of a medicinal composition consisting of the Notch pathway inhibitor and an mTOR pathway inhibitor in preparation of a medicament for treating tumors of mammals comprising human beings due to activation of an mTOR. The application provides a new path for the treatment of the tumors caused by the activation of the mTOR.
EP1560587A1 Cholesterol efflux and uses thereof In a first aspect of the present invention, there is provided a method of modulating cholesterol efflux in a cell, said method comprising modulating expression and/or activity of sterol 27-hydroxylase (CYP27) and/or caveolin-1 in the cell. Applicants have found that cholesterol can be removed by cholesterol efflux which is regulated by CYP27 and/or caveolin-1. More suprisingly for CYP27 modulation the cholesterol effluxed remains in the form of cholesterol and not as oxidized cholesterol as would be expected in the presence of CYP27. Preferably, CYP27 is modulated in macrophages and caveolin-1 is modulated in hepatic cells.
CN1562055A Medicinal composition for treating liver disease A composite medicine for treating hepatitis, hepatofibrosis, heptocirrhosis, hepatoascites and liver cancer is proportionally compound of arasaponin and the kuhseng alkaloid chosen from the common alkaloid of kuhseng, common alkaloid of subprostrate sophora, common alkaloid of sophora alopecuroids, matrine and kurannol.
EP2201950A1 Compounds and methods for treating autism spectrum disorders The present invention relates to a compound of the following formula (I): or a pharmaceutically acceptable salt thereof, for use in the prevention or treatment of autism spectrum disorders (ASD).
CN101283981A Sustained-release injection containing antibiotic The invention provides a sustained-release injection or sustained-release implant containing antibiotics. The sustained-release injection comprises sustained-release microspheres and solvent. The microspheres contain sustained-release adjuvants and antibiotics, and the solvent is a special solvent containing suspending agent such as sodium carboxymethylcellulose and having viscosity of 100-3000cp (20-30 DEG C); and the sustained-release adjuvants are selected from poly(ethylene-co-vinylacetate) (EVAc), polifeprosan, poly(lactic acid) (PLA), poly(lactic-co-glycolic acid) (PLGA), sebacic acid copolymer, albumin glue and gelatin. The sustained-release implant is made from microspheres or by other methods. The sustained-release implant or injection can be locally placed or injected into foci to locally sustained-release the drug for more than 10 days, so as to obtain and maintain local drug effective concentration while remarkably reduce the systemic toxicity of the drug. The sustained-release injection has distinct and unique therapeutic effect on local infection diseases caused by Staphylococci, Streptococci, Peptostreptococcus, Propionibacterium acnes, Enterobacter, Mycobacterium tuberculosis, Gonococcus or Meningococcus, such as chronic osteomyelitis, severe decubital ulcer, refractory skin ulcer, diabetic foot, femoral head necrosis and abscess.
WO2013171334A1 Methanethione compounds having antiviral activity A compound of formula (I), The compound is useful as an antiviral agent, in particular for the treatment of influenza. A method for preparing the compound of formula (I) and a composition comprising the compound of formula (I).
CN101259106A Nano controlled release compositions comprising a cephalosporin The present invention provides a composition comprising cephalosporin useful in the treatment and prevention of a bacterial infection. In one embodiment, the composition comprises nanoparticulate particles comprising cephalosporin and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. In another embodiment, the composition comprises a modified release composition that, upon admiriistration to a patient, delivers cephalosporin in a bimodal, multimodal or continuous manner. The invention also relates to dosage forms containing such compositions, and to methods for the treatment and prevention of a bacterial infection.
US20100137315 Sphingosine Kinase Inhibitors and Methods of Their Use The invention relates to compounds, pharmaceutical compositions thereof, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
WO2008055445A1 Method and composition for increasing insulin sensitivity The present invention provides a use of SIRT1 protein or agonists or up-regulators thereof for manufacturing a composition which can increase insulin sensitivity. SIRT1 can be used to increase insulin sensitivity by down-regulating expression of protein tyrosine phosphatase 1B, a negative regulator of insulin action.
WO2006115238A1 Gastrointestinal motor activation regulator A highly safe pharmaceutical having an excellent gastrointestinal motor activation-regulating effect is provided. It is a gastrointestinal motor activation regulator comprising methylmethionine sulfonium chloride, which can be used as an excellent gastrointestinal motor activation regulator having a high pharmacological action and no side effects.
US20110076243 Modified hydrophilic polymers containing hydrophobic groups Disclosed are hydrophilic polymers such as polysaccharides, including hyaluronic acid of any origin, modified by reaction with epoxy-functional-silicones. Hydrophobic silicon, which contains chemically active groups covalently attach to the backbone of the hydrophilic polymer and gives these new, modified polymers the ability to dissolve hydrophobic compounds including oils, drugs, and vitamins, while maintaining the hydrophilic properties and benefits of the unmodified polymer. With respect to topical applications these polymers substantially increase the stability of formulations and provide for ease of preparation. The properties and advantages of the original polymer are maintained while other properties are augmented, namely the ability to combine with or dissolve hydrophobic and hydrophilic drugs. The products can be used alone or in combination with other substances for various applications including cosmetic, medical, and drug delivery applications. Also disclosed are methods for preparing them.
CN101805290A Aminosulfonyl pyrazol compounds and applications thereof The invention relates to aminosulfonyl pyrazol compounds shown in a general formula (I) and pharmaceutically acceptable salts thereof, wherein n is integer of 1-6, R1 is C1-C9 alkyl, C3-C7 fat ring or heterocyclic ring, halogen, nitryl, C1-C6 alkyl, C1-C6 alkoxyl substituted or unsubstituted phenyl, naphthyl and heteroaromatic ring containing 1-3 heteroatoms; R2 is hydrogen; and R3 is hydrogen or CO2H. The aminosulfonyl pyrazol compounds or pharmaceutically acceptable salts thereof can be applied to the aspects of allaying a fever, relieving pain and resisting inflammation and preventing and treating tumors.
US20100069473 Inhibitors Of IKK-Beta Serine-Threonine Protein Kinase Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; Y1 is a bond, —(C═O)—, —S(O2)—, —C(═O)O—, —OC(═O)—, —(C═O)NR3—, —NR3(C═O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C═O)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims.
WO2006102333A2 Ophthalmic use of agents which inhibit connective tissue growth factor binding and signalling via the trka/p75ntr receptor complex The present invention provides a method for lowering intraocular pressure and providing neuroprotection to a patient in need thereof by administering a therapeutically effective amount of at least one agent that inhibits binding and/or signaling of connective tissue growth factor (CTGF) via the TrkA/p75NTR receptor complex. In a preferred embodiment, the present invention relates to the use of the tyrosine kinase inhibitor K-252a in the treatment of CTGF-mediated ocular disorders like glaucomas.
US20090192102 miR-21 REGULATED GENES AND PATHWAYS AS TARGETS FOR THERAPEUTIC INTERVENTION The present invention concerns methods and compositions for identifying genes or genetic pathways modulated by miR-21, using miR-21 to modulate a gene or gene pathway, using this profile in assessing the condition of a patient and/or treating the patient with an appropriate miRNA.
CN103202871A Externally-applied medicine patch for dehydration and detumescence, and production method of same The invention discloses an externally-applied medicine patch for dehydration and detumescence, and a production method of the same. The externally-applied medicine patch for dehydration and detumescence is prepared from the raw material medicines in parts by weight: 400-650 parts by weight of magnesium sulphate, 20-45 parts by weight of calcium gluconate, 30-100 parts by weight of semen celosiae, and 30-100 parts by weight of mustard seeds. The production method for the externally-applied medicine patch comprises the following steps of: preparing magnesium sulphate and calcium gluconate into powder, and uniformly mixing and stirring the magnesium sulphate powder and the calcium gluconate powder with semen celosiae and mustard seeds to obtain a mixture; and sewing a line on two cloth sheets at an interval of 1-2 cm to form strip-shaped gaps, sewing a line at one end of each strip-shaped gap, filling the externally-applied medicine mixture in the strip-shaped gap at the other end of the strip-shaped gap, and then cutting and sewing to obtain an externally-applied medicine patch shape easy to externally apply each part of a human body. The externally-applied medicine patch for dehydration and detumescence disclosed by the invention has the effects of dehydration, dryness, detumescence and pain relief, and is capable of drying all the focuses of human body to achieve the purpose of eliminating the focuses. The externally-applied medicine patch for dehydration and detumescence has a great treatment effect on tumour, rheumatic joint pains, cervical bone hyperplasia, lumbar bone hyperplasia, lumbar disc herniation, hypertension, lung diseases and the like.
US7544677 Cancer; 2-(methylthio)-6-phenyl-7-(4-{[4-(5-pyridin-2-yl-4H-1,2,4-triazol-3-yl)piperidin-1-yl]methyl}phenyl)pyrido[2,3-d]pyrimidine;serine/threonine kinase (Akt) suppression; increased cellular potency or solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
CN1903198A Kurarinol slow-release dripping pills for treating hepatitis B A slow-release dripping pill of kurarinol for treating hepatitis B is prepared from kurarinol and proper matrix proportionally through proper process.
CN103372008A Application of Chukrasone B in the preparation of anti-herpes virus medicines The invention discloses an application of Chukrasone B in the preparation of anti-herpes virus medicines. Experiments prove that the Chukrasone B has an obvious inhibiting effect on anti-herpes simplex virus-1 (HSV-1) and anti-herpes simplex virus-2 (HSV-2), thus showing that the Chukrasone B has potential application value in the field of herpes virus infectious disease treatment. The application of the Chukrasone B provides an experimental basis for the clinic application of the Chukrasone B in the treatment of herpes virus infectious diseases and certain guiding significance for the development of the anti-herpes virus medicines and has important reference value.
CN101933902A Granisetron hydrochloride microemulsion-based gel and preparation method thereof The invention discloses a granisetron hydrochloride microemulsion-based gel and a preparation method thereof. The preparation contains microemulsion and blank gel, wherein the microemulsion consists of granisetron hydrochloride or free alkali thereof, oil phase, emulsifier, co-emulsifier and water phase; and the blank gel consists of gel matrix, neutralizer, humectant and water. The preparation method of the preparation uses the conventional pharmaceutical equipment and comprises the following steps: evenly mixing microemulsion and blank gel in a certain ratio, adding a certain amount of penetration enhancer, and adjusting the pH value to obtain the granisetron hydrochloride microemulsion-based gel. The preparation has simple preparation technology, high production efficiency, low cost, stable quality and easy industrial production. The product of the invention has good effect of transdermal absorption, hardly has any stimulation on the skin and can satisfy the clinical medication requirements basically, thus the product is a novel preparation with good compliance and high therapeutic index.
CN101906101A Rotundine crystal B-type solid matter and preparation method as well as applications The invention discloses a novel crystal-type state of rotundine solid chemical matter, which is shown as the formula (I), a preparation method of the novel crystal-type sample, and superior clinical therapeutic action of the novel crystal-type matter of the rotundine as active components in the preparation and the development of various formulations and medicament compositions for preventing and treating pains caused by various reasons, including headache, cramp, labour pains, and the like, and diseases caused by pains, such as insomnia, arrhythmia, and the like. Compared with the traditional officinal crystal-type solid matter (Crystal A type), the two types of novel crystal-type solid matter of the rotundine have higher absorption and blood concentration. Different crystal-type matter can influence the absorption speed and the blood concentration in an organism as well as the bioavailability of the active components of the medicaments, and thereby influencing the preventive and therapeutic effect of the medicaments in clinical applications.
US20110021469 baclofen solution for low-volume therapeutic delivery A high concentration baclofen solution is provided suitable for therapeutic use in a medical setting. A high concentration solution of baclofen in multivalent physiological ion solution such as artificial cerebrospinal fluid is provided with concentrations of baclofen of 10 mg/ml. Artificial cerebrospinal fluid is particularly advantageous as a baclofen solvent. A medical package is also provided for baclofen delivery to patients suffering from spasticity.
CN1861100A External use oil agent for treating proliferation of mammary gland and its prepn. method An exterior-applied ointment for preventing and treating mastoplasia by coating it on breast and massaging is prepared from the twig and leaf of enqlish yew, taxol, safflower, red sage root and burreed tuber. Its preparing process is also disclosed.
WO2007062805A1 3-(SUBSTITUTED AMINO)-PYRAZOLO[3,4-d]PYRIMIDINES AS EPHB AND VEGFR2 KINASE INHIBITORS The invention relates to novel pyrazolo[3,4-d]pyrimidines of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
US20120045516 Composition for photodynamic therapy comprising a macromolecular capsule A composition for photodynamic therapy including a polymer capsule having a diameter of about 10 nm to about 2000 nm synthesized by copolymerization of a flat aromatic compound represented by Formula 1 (see the specification) and an organic compound represented by Formula 2 (see the specification).
CN101862341A Application of Spinosad for wound healing The invention discloses application of Spinosad, or physiologically acceptable derivatives or salts thereof for promoting or accelerating wound healing of a human.
CN102921015A Hyaluronic acid nanometer selenium and preparation method as well as application thereof The invention discloses hyaluronic acid nanometer selenium and a preparation method as well as application thereof, belonging to the technical field of nanometer medical materials. According to the hyaluronic acid nanometer selenium, hyaluronic acid is used as a carrier, sodium selenite is used as a raw material, red spherical hyaluronic acid nanometer selenium is prepared by taking ascorbic acid as a reducing agent under a room temperature condition, and the particle size is 50-70 nm. The hyaluronic acid nanometer selenium prepared by adopting the method has the advantages of small particle size, narrow particle size range, good dispersibility and the like, can still remain stable for a month at room temperature, has a mild reaction condition, is easy to operate and is an environment-friendly synthesis method; and some defects, such as wide particle size range, poor dispersibility and poor stability, existing in the conventional preparation are overcome. The hyaluronic acid nanometer selenium has an obvious inhibition effect on growth of HepG-2 liver cancer ascites tumor cells implanted in the body of a mouse, and can be used as an anti-tumor auxiliary medicament or a health-care product for improving the immunologic function of the body.
WO2009027105A2 Method of providing patient specific immune response in amyloidoses and protein aggregation disorders A novel treatment of Alzheimer's disease and other disorders involving protein misfolding or aggregation is provided by enhancing or sustaining an antibody response against predominantly directed against pathological protein aggregates or neo-epitopes present on pathogenic forms of said protein or protein complex. Furthermore, therapeutic methods are described, wherein ex vivo stimulated antigen-selected peripheral blood lymphocytes are regrafted into the cognate donor.
EP2766364A1 Folate conjugates of albumin-binding entities The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.
US20080171786 Substituted [(Phenylethanoyl)Amino]Benzamides The invention relates to substituted [(phenylethanoyl)amino]benzamides and methods for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of inflammatory disorders such as, for example, cutaneous, respiratory tract and cardiovascular disorders such as, for example, arteriosclerosis and coronary heart disease.
WO2006085688A1 Psychogenic pain therapeutic agent It is intended to provide a psychogenic pain therapeutic agent that exerts an excellent therapeutic effect on psychogenic pain which is an intractable disease. More specifically, it is intended to provide a psychogenic pain therapeutic agent comprising a phenylethanolamine N-methyl transferase (PNMT) inhibitor such as DCMB ((±)-2,3-dichloro-α-methylbenzylamine) as an active ingredient, a pharmaceutical composition for psychogenic pain therapy comprising the PNMT inhibitor as an active ingredient, and a therapeutic method for psychogenic pain using the PNMT inhibitor.
CN102227217A Methods and compositions for improving cognitive function This invention relates to treating age-related cognitive impairment. This invention in particular relates to the use of inhibitors of synaptic vesicle protein 2A (SV2A), such as levetiracetam, seletracetam, and brivaracetam, in improving cognitive function in subjects that exhibit age-related cognitive impairment or are at risk thereof, including, without limitation, subjects having or at risk for Mild Cognitive Impairment (MCI), Age-related Cognitive Decline (ARCD) or Age-Associated Memory Impairment (AAMI).
US20050222420 Chain oligolactic acid thioester An object of the present invention is to produce and isolate a linear oligolactic acid thioester having a thioester group at the terminus as a single compound. According to the present invention, there is provided a compound represented by the formula (1) or a salt thereof: wherein X represents a hydrogen atom or a protective group for a hydroxyl group; Y represents an aliphatic group, an aryl group or a heterocyclic group; and n represents an integer of 0 to 19.
CN103417817A TCM composition for treatment of upper respiratory infection and acute tonsillitis in children The invention relates to TCM composition for the treatment of upper respiratory infection and acute tonsillitis in children. The TCM composition is made with 4.76g of artificial cow-bezoar, 9.52g of pearl, 23.81g of realgar, 47.62g of Chinese rhubarb, 23.81g of coptis root, 17.86g of licorice root, 47.62g of snakegourd root, 23.81g of unibract fritillary bulb, 47.62g of red peony root, 23.81g of prepared frankincense, 23.81g of prepared myrrh, and 5.95g of borneol. The realgar is made into superfine powder by elutriation; the pearl and borneol are made into superfine powders by low-temperature crushing; other materials expect the artificial cow-bezoar are mixed and crushed into fine powder; the superfine powders of the artificial cow-bezoar, realgar and the like are mixed well and are then mixing well with the fine powder obtained by mix-crushing; the mixture is made into capsules, tablets and pills. The TCM composition is even in ingredient content, effective ingredients are retained completely, efficacy of the composition is enhanced, and the composition has no toxic and side effects and is safe to apply.
WO2011135355A1 3-{ [5 -(azetidin-1-ylcarbonyl)pyrazin-2 -yl] oxy} -5-{ [(1s) -2 -hydroxy- 1 -methylethyl]oxy} -n- (5 -methylpyrazin-2-) benzamid monohydrate Crystalline 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-2-hydroxy-1- methylethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide monohydrate is an activator of glucokinase (GLK or GK) and is useful as a pharmaceutical compound in the treatment of 5 diabetes and/or obesity. Processes for the manufacture of this crystalline form, pharmaceutical compositions comprising the crystalline form and the use of the crystalline form in medical treatment are also disclosed.
CN101591368A Girald pteroxygonum root neoflavonoid compound The invention provides a girald pteroxygonum root extract with structure shown in formula (I), a neoflavonoid compound with structure shown in formula (I), an extract containing the compound in formula (I) and a preparation method of the neoflavonoid compound and a medical application in treating diseases related to free radicals therewith.
CN102525880A Aprepitant solid dispersion composition The invention belongs to the field of medicinal preparation, and particularly provides an aprepitant solid dispersion composition and a preparation method thereof as well as a medicinal composition prepared from the solid dispersion composition. The composition contains aprepitant and at least one water-soluble polymer, and the aprepitant is uniformly dispersed in the water-soluble polymer. The mass ratio of the aprepitant to the water-soluble polymer is 1:(0.5-10). The aprepitant solid dispersion composition provided by the invention is dissolved in a water-based medium at an unexpected high level in a relatively short time, and has the advantages of improved dissolution characteristic and obvious physical stability.
WO2013167303A1 Sugar compositions for treating hemophilia a and/or von willebrand disease The invention relates to compositions comprising an isolated sugar for use in the treatment of von Willebrand disease and/or hemophilia A, wherein the sugar is an accessible sugar residue derived from ABO(H)blood group antigen.
EP1863534A1 Composition comprising a combined thromboxane receptor antagonist and thromboxane synthase inhibitor and a cox-2 inhibitor The invention relates to a pharmaceutical composition comprising a combined thromboxane receptor antagonist and thromboxane synthase inhibitor and a COX-2 inhibitor. In addition a method of treating cyclooxygenase dependent disorders, including inflammation, pain and/or rheumatic diseases, and/or neoplasia is described.
WO2008031569A1 Means for increasing intracellular levels of protoporphyrin ix and use thereof The present invention is related to a nucleic acid molecule comprising a double-stranded structure, whereby the double-stranded structure comprises a first strand and a second strand, whereby the first strand comprises a first stretch of contiguous nucleotides and the first stretch is at least partially complementary to a target nucleic acid, and whereby the second strand comprises a second stretch of contiguous nucleotides and whereby said second stretch is at least partially complementary to the first stretch, whereby the first stretch comprises a nucleic acid sequence which is complementary to a nucleotide sequence starting from position 383, 1013 or 1982 of the nucleic acid according to SEQ.ID.No. 1.
EP1087768B1 Use of 1-(aminoalkyl)-3-quinoxaline-2-one derivatives for the preparation of compounds having an antioxidant action The invention relates to the use of 1-(aminoalkyl)-3-quinoxaline-2-one derivatives, especially 1-diethylaminoethyl-3-quinoxaline-2-one derivatives of the formula (I), where R3 is hydroxy, methoxy, ethoxy or hydrogen, or pharmaceutically compatible salts thereof, for the preparation of compounds having an antioxidant action and used for preventing or treating diseases caused by free radicals of the cellular oxygen metabolism, stimulating nerve cell growth, antagonizing glutamate receptors and/or stimulating the growth notably of glutamergic nerve cells.
US20110053933 Hydroxyquinoxalinecarboxamide derivative The present invention provides a novel hydroxyquinoxaline carboxamide derivative that is useful for preventing and/or treating blood coagulation disorders. A compound represented by formula (i), or a pharmacologically acceptable salt thereof: wherein, each of R1 and R2 independently represents a group such as a hydrogen atom or a halogen atom; R3 represents a group such as a hydrogen atom; each of R4 and R5 independently represents a group such as a hydrogen atom, a halogen atom or a C1-4 alkyl group; each of R6 and R7 independently represents a hydrogen atom or a C1-4 alkyl group; X represents a group such as a C3-10 cycloalkyl group, C6-10 aryl group or a 5- to 10-membered heterocyclic group, which may be substituted with substituent(s) selected from substituent group α; Y represents a group such as —CO—, —O— or —NRa—, and Ra represents a group such as a hydrogen atom or a C1-4 alkyl group.
CN101747345A Amorphous cefodizime sodium and preparation method thereof and pharmaceutical composition comprising same The invention provides an amorphous cefodizime sodium, which is characterized in that an amorphous X-ray diffraction pattern is free from having an X-ray diffraction peak; and in an amorphous differential thermogram, the endothermic peak stays at 57 to 68 DEG C, and the exothermic peak stays at 250 to 258 DEG C. The organic residual value in the cefodizime sodium is low, so the cefodizime sodium is free from entering into a hard lamp during the drying and is easy to operate; the obtained product presents in an apparent granular shape, and the fluidity is good; and when the cefodizime sodium is used for the preparation, the cefodizime sodium is free from being crushed and can be directly homogenized to be prepared, thereby saving device, power and labor cost for the industrialized production, and shortening the production period.
CN101031283B Pharmaceutical compositions for drug delivery The present invention relates to pharmaceutical compositions in the form of a gel for controlled- or sustained- release of a pharmaceutically active agent and to methods for treating or preventing or preventing a condition in an animal by administering to an animal in need thereof the pharmaceutical compositions. One particular type of condition for which the pharmaceutical compositions are useful is a microbial infection, e.g., of the skin, ear, or eye, especially for veterinary applications.
US20060057628 Method for prognosticating the progress of breast cancer and compounds useful for prevention or treatment thereof This invention concerns in vitro method for prognosticating the progress of breast cancer, comprising detecting or quantifying the level of 17β-hydroxysteroid dehydrogenase (17HSD) type 1 enzyme in breast tumor tissue sample, wherein the presence of said 17HSD type 1 enzyme is indicative of severe progress of breast cancer. Furthermore, the invention also concerns the use of a 17HSD type 1 enzyme inhibitor for prevention or treatment of breast cancer. This invention concerns also the use of compound A in the manufacture of a pharmaceutically acceptable preparation useful as 17HSD inhibitor.
CN1990447A Keton of Gentianopsis Paludosa Ma and its derivative, and preparing method and use thereof The invention relates to biological chemical compound, which in detail relates to fluorenone and its derivative as well as its preparation and application. The chemical structural general formula is showed in (1), and R1, R2 and R3 are H or -CH3. The compound is characterized by function of anti-oxidation, anti-bacteria and smooth muscle relaxation, and it is can be used to prepare medical compound, especially anti-oxidation agent for food, anti-bacteria agent for plant and calcium ion antagonist and so on.
US20080249088 consisting of benzylamine derivatives and morpholine derivatives; an aliphatic alcohol substituted with an aromatic substituent in which the antifungal compound is soluble to a therapeutically effective concentration; can be applied topically in solution; and a distribution solvent A topical formula for treatment of antifungal infections of the skin and nails comprises: (a) a therapeutically effective amount of a benzylamine or morpholine antifungal compound; (b) an aliphatic alcohol substituted with an aromatic substituent in which the antifungal compound is soluble to a degree that a therapeutically effective concentration of the antifungal compound can be applied topically in solution; and (c) a distribution solvent or mixture of solvents in which the solvent mixture of parts (a) and (b) is soluble, and which has a boiling point that is less than about 110.degree.C. The benzylamine compound can be butenafine. The morpholine compound can be amorolfine. The aliphatic alcohol substituted with an aromatic substituent can be benzyl alcohol, or phenethyl alcohol. The distribution solvent mixture can include ethyl alcohol, water, or isopropyl alcohol. Alternatively, the formula can include a second antifungal compound.
WO2012092712A1 Lyophilized nanometer particle powder preparation comprising recombinant albumin prepared from human plasma A lyophilized nanometer particle powder preparation comprising recombinant albumin prepared from human plasma and the preparation method thereof. Said preparation consists of docetaxel, phospholipid, recombinant albumin prepared from human plasma, support agent for lyophilization, pH regulator and a small amount of water, wherein the average diameter of the particle is less than 0.4 μm, and the mass percent of each composition is as follows: docetaxel 0.05-5%, phospholipid 0.1-50%, recombinant albumin prepared from human plasma 1-60%, support agent for lyophilization 1-60%, pH regulator 0.05-10% and the small amount of water is less than 5%. The powder preparation, injection water, glucose and saline are remade to an injectable aqueous solution with pH of 5.0-7.0.
CN101362757A Sulfonyl substituted carbpenems compounds The invention pertains to the technical field of medicine and particularly relates to a compound shown as general formula (I), and pharmaceutically acceptable salts, easily hydrolysable ester, isomers and hydrates of the compound, as well as hydrates of the ester or the salt of the compound; wherein, R<1>, R<2>, R<3> and A are defined as the specification. The invention also relates to a preparation method of the compounds, medicine composition containing the compounds as well as application of the compounds to the preparation of medicines treating and/or preventing infectious diseases.
CN103450079A Tetrahydroisoquinoline hydroxyl derivate, preparation method and medical application thereof The invention belongs to the field of medicinal chemistry, and particularly relates to a tetrahydroisoquinoline hydroxyl derivate, a composition containing the hydroxyl derivate, and application of the derivate or composition serving as a kappa-opioid receptor agonist for analgesia. The pharmacodynamic test result shows that the compound has high analgesia effect, can obviously reduce central sedation and anxiety side effects, and overcomes the side effect of the existing analgesics.
CN101695516A Immunostimulant for aquatic animals and preparation method thereof The invention provides an immunostimulant for aquatic animals and a preparation method thereof. The immunostimulant for the aquatic animals consists of the following components in part by weight: 150 to 250 parts of milkvetch, 150 to 250 parts of liquorice, 100 to 200 parts of mongolian dandelion herb, 200 to 300 parts of yeast, 30 to 80 parts of spirulina, and 100 to 200 parts of glucosan. The preparation method thereof comprises the steps of: taking the milkvetch, the liquorice and the mongolian dandelion herb for micronization, then adding the yeast, the spirulina and the glucosan, and stirring the mixture evenly to obtain the immunostimulant. The immunostimulant for the aquatic animals can obviously improve the immunity and disease resistance of the aquatic animals, effectively lower the death rate of the aquatic animals caused by various factors, can promote the growth of organisms and improve the survival rate of the organisms and the utilization rate of feed; and the preparation method thereof is simple and suitable for the need of mass industrial production.
WO2007066928A1 Use of the extract of caesalpinia sappan l. and compounds therefrom The present invention relates to an extract of Caesalpinia sappan L. having an angiogenesis inhibition activity and a use of the compound isolated therefrom, more precisely an extract of Caesalpinia sappan L. extracted by using water, alcohol or a mixture thereof , and a use of brazilin, sappanchalcone and brazilein isolated from the extract as an angiogenesis inhibitor. The extract of Caesalpinia sappan L. of the invention and a compound isolated therefrom have angiogenesis inhibition activity, so that they can be effectively used for the prevention and treatment of angiogenesis associated diseases such as vascular diseases, cardiovascular diseases, ophthalmic diseases, chronic inflammatory diseases, dermatological diseases, Alzheimer's disease, obesity and cancer.
EP1584333A2 Use of acetylcoenzime A inhibitors for treating Alzheimer's disease The present invention provides a method for treating or preventing the onset of Alzheimer's Disease comprising administering to a mammal in need thereof an Alzheimer's Disease-preventing or treating amount of a plasma-triglyceride level-lowering agent. Optionally, the plasma-triglyceride level-lowering agent can be co-administered with a cholesterol level-lowering agent.
US20120035107 Compositions for achieving a therapeutic effect in an anatomical structure Compositions and methods of using the compositions are provided for forming an embolus within a region of an anatomical lumen for a transitory period in order to achieve a therapeutic effect.
CN1990475B Substituted benzisoselenazolone compounds and use thereof The invention relates to a subsitituent benzisoselenazolone derivative with general formula (I) or (II) of anti-inflammatory, anti-tumor or anti thrombus, medical compound containing said derivative, and its application for preparing drug than can treat inflammatory, tumor or thrombus formation.
CN103751203A Medicinal composition for treating essential hypertension and application thereof The invention belongs to the technical field of medicine, particularly relates to a medicinal composition for treating essential hypertension and application thereof. The medicinal composition is prepared from the following raw materials: Lycium barbarum polysaccharide component II, Lycium barbarum polysaccharide component III, friedelin-3beta-ol, Astragalus polysaccharide component A1 and Ajugol A. The medicinal composition provided by the invention has obvious therapeutic effect of inhibiting clinical symptoms of essential hypertension, has the advantages of stable quality control, no toxicity and is suitable for long-term administration.
CN102872038A Application of Gypensapogenin B in medicaments against herpes viruses The invention discloses an application of Gypensapogenin B in preparing medicaments against herpes viruses. Experiments show that Gypensapogenin B has notable inhibiting actions against Herpes simplex virus 1 (HSV-1) and actions against Herpes simplex virus 2 (HSV-2), which prompts that Gypensapogenin B has potential application value in the filed of treating herpes virus infectious diseases. The invention provides an experimental base for the clinical application of Gypensapogenin B in treating herpes virus infectious diseases, has certain guide significance for developing medicaments against HSV-1 and HSV-2, and has important reference value.
CN102600248A External medicine for treating toothache The invention provides external medicine for treating toothache. The medicine is characterized by consists of the following raw material medicine in weight: 25g of alum and 120g of fresh snakeweed. A preparation method of the medicine comprises the following steps that: the alum is crushed and is screened by a sieve being 80 meshes, the snakeweed is cleanly washed, the alum and the snakeweed are uniformly mixed and are mashed into juices to be dripped into the auditory meatus. The medicine has the efficacies and beneficial effects that the alum is cold in property and is acerb in taste, a strong convergence effect is realized, and the efficacies of eliminating toxin, killing intestinal worms, removing dampness, relieving itching, stopping bleeding, stopping diarrhoica, clearing away the heat and dissolving the phlegm are realized. The alum also has antibacterium effect, anti-trichomonas-vaginalis effect and the like. The snakeweed has the effects of clearing away the heat, realizing diuresis, cooling the blood and eliminating the toxin. The medicine mainly treats heat accumulation of the bladder, dysuria, leucorrhea, summer damp diarrhea, nosebleed, hematuria, liver heat and hot eyes, swelling and pain in throat and swollen welling-abscess toxin and has the anti-inflammatory effect. The external medicine has the advantages that the preparation is simple, the side effect is small, and the external medicine is applicable to various kinds of toothache.
EP1158872B1 Dietary compositions and methods Dietary compositions and methods employ a mammal food base and a component comprising estrogen, androgen or a mixture thereof in an amount sufficient to reduce weight gain normally incurred in the mammal type subsequent to neutering, castration, spaying, ovariectomy or ovariohysterectomy, or post menopause. Preferably, the component comprises phytoestrogen, phytoandrogen or a mixture thereof. The compositions are adapted for administration to the mammal on a regular, preferably daily, basis.
US20110014192 Suppression of cancer growth and metastasis using nordihydroguaiaretic acid derivatives with metabolic modulators Disclosed is a composition comprising a derivative of NDGA and at least one metabolic modulator. The composition can be in a unit dose form or kit. The composition can comprise at least two metabolic modulators. Also disclosed are methods for achieving cytotoxicity, particularly of rapidly dividing cells such as cancer, by administering a composition of the invention. In various embodiments of the invention subjects with cancer achieve prolonged survival and/or diminution in the size of their malignancies and cancer metastasis.
US20110110933 Ectopic pregnancy treatment The invention pertains to methods for treating ectopic pregnancy. More particularly, the present invention relates to methods for treating unruptured ectopic pregnancy using a non-surgical method comprising the administration of an EGFR inhibitor alone or in combination with an anti-metabolite e.g. methotrexate (MTX). The methodology is potentially applicable to treatment of unruptured ectopic pregnancies of all sizes.
US20120202795 Substituted pyridones as inhibitors of poly(adp-ribose) polymerase (parp) The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.
CN103239459A Use of sterol derivative in preparation of medicines for preventing and/or treating and/or adjunctively treating cancers The invention discloses a sterol derivative, and provides a use of the sterol derivative in the preparation of medicines for preventing and/or treating and/or adjunctively treating cancers. The sterol derivative comprises sterol compounds having a structural formula (I), pharmaceutically acceptable salts of the sterol compounds, extract products including the sterol compounds, or compositions including the sterol compounds. In the structural formula (I), R1 is -OH, =O, H, or a C1-C3 alkyl group; R2 is -OH, H, or a C1-C3 alkyl group; R3 is -OH, =O, H, or a C1-C3 alkyl group; R4 is -OH, H, or a C1-C3 alkyl group; and at least one of R1, R2, R3 and R4 is -OH. The compounds having the structural formula (I) can be used for preparing anticancer medicines, and the anticancer effects of the prepared anticancer medicines are good.
US20050119323 Hormone sensitive vcancer; antiproliferative agents ; induction apoptosis; angiotensin inhibitors Remedies/preventives for hormone-independent cancer, hormone-independent cancer cell proliferation inhibitors, apoptosis inducers for cancer cells, etc. each containing a compound having an angiotensin II antagonism, its prodrug or a salt thereof. Thus, excellent anticancer agents are provided.
CN1730476B Aromatic amine ketone compounds, its synthesis method, pharmaceutical composition containing same and uses The invention provides arylamine ketone compounds having a general formula (I), the preparation of the compound, the medicinal composition containing them and the use of these compounds in preventing and/or treating platelet activating factor related diseases, especially the use in antiphlogistic immunization, in particular for treating acute or chronic inflammation, such as osteoarthritis, chronic infectious arthritis etc.
US20110305633 Methods for Treatment, the Prognostic Assessment and the Detection of Breast Cancer The present invention relates to methods for the treatment, the prognostic assessment and the detection of breast cancer.
US20100047307 Injectable drug carrier comprising layered double hydroxide Provided is an injectable drug carrier including a non-toxic Layered Double Hydroxide (LDH) and pharmaceutically acceptable excipients. Provided is also a method of preparing the injectable drug carrier, the method including: synthesizing LDH with various compositions and controlling the size and shape of the LDH at a level that the LDH has no adverse effect in vivo. A solution obtained by dispersing the LDH in a solvent is injected in vivo. According to the method, nano-size LDH that does not affect a blood vessel in vivo can be synthesized. The LDH thus synthesized has no adverse effect in vivo even at a concentration of 400 mg/kg, and thus can contribute to establishment of a drug delivery system capable of improving the delivery efficiency of a specific drug.
EP1523556A1 Methods of treating conditions associated with an edg-1 receptor In one aspect, the present invention provides a method of modulating an Edg-1 receptor mediated biological activity in a cell. A cell expressing the Edg-1 receptor is contacted with a modulator of the Edg-1 receptor sufficient to modulate the Edg-1 receptor mediated biological activity. In another aspect, the present invention provides a method for modulating an Edg-1 receptor mediated biological activity in a subject. A therapeutically effective amount of a modulator of the Edg-1 receptor is administered to the subject.
WO2014075387A1 Diaryl hydantoin derivative, and preparation method, pharmaceutical composition and use thereof Provided are a compound as represented by formula I, or pharmaceutically acceptable salt, solvate, precursor drug, stereoisomer, tautomer, polymorph or metabolite thereof, pharmaceutical composition containing same, and uses thereof in the preparation of drugs for treating androgen receptor related diseases.
CN101244220A Black thorn chinaroot greenbrier total saponin extract and preparation thereof The invention discloses an extraction of total saponins extracted from blackthorn chinaroot greenbrier and the preparation method, wherein, the extraction mainly comprises saponins a and saponins b of blackthorn chinaroot greenbrier as well as the analogues; the extraction can be prepared with one of solvent extraction method, macroporous rosin adsorption method, supercritical fluid extraction method, column chromatography method, liquid-liquid countercurrent distribution chromatography or the random combination of the methods; the content of total saponins in the extraction of total saponins of blackthorn chinaroot greenbrier is totally 5 to 100% (W/W), wherein, the total content of saponins a and saponins b of blackthorn chinaroot greenbrier as well as the analogues is 5 to 100% of the content of total saponins in weight ratio.
CN1875957A A nano antibacterial medicine of furacillin and preparation method thereof The invention discloses an antibacterial drug of nitrofurazone nano emulsion for anti-inflammation of human and animal skin and mucous membrane, and is prepared from nitrofurazone 0.01-1.00% as the medicinal constituent, nano emulsion matrix 69.99-99.85% and auxiliary material 0.10-30.00% through mixing proportionally and stirring homogeneously.
WO2014160197A1 Thiazole compounds, compositions and methods for treatment of degenerative diseases and disorders Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
WO2013134230A1 Boron-based 4-hydroxytamoxifen and endoxifen prodrugs as treatment for breast cancer The present disclosure relates to boron-based 4-hydroxytamoxifen and endoxifen prodrugs and the synthesis of the same. Further, the present disclosure teaches the utilization of the boron- based 4-hydroxytamoxifen and endoxifen prodrugs in a treatment for breast cancer.
US20110104147 Identification of Tumor-Associated Markers for Diagnosis and Therapy The present technology relates to genetic products the expression of which is associated with cancer diseases. The present technology also relates to the therapy and diagnosis of diseases in which the genetic products are expressed or aberrantly expressed, in particular cancer diseases.
CA2171625C Oxidized carotenoids, retinoids and related conjugated polyenes, and derived fractions and compounds useful as cell-differentiation inducers, cytostatic agents, and anti-tumor agents .beta.-Carotene, lycopene and canthaxanthin, as represented by carotenoids, retinoic acid, and representative retinoids, undergo extensive oxidation to yield substances which have properties useful as non--toxic agents active against cell proliferation, tumors, and tumorigenic viruses, and useful as promoters of cell differentiation. It is evident from chemical analysis of the highly oxidized .beta.-carotene product mixture that none of the various forms of vitamin A are present or are present only in minor amounts. Furthermore, the biological activities of oxidized canthaxanthin and lycopene indicate the presence of active substances that are different from vitamin A. Although the cytostatic and differentiation promotion activities of oxidized .beta.-carotene resemble those of vitamin A itself, generally the effects are more powerful for oxidized .beta.-carotene in a wide variety of circumstances. Unlike vitamin A, the oxidized .beta.-carotene of the invention is non-toxic. The oxidized carotenoid is a mixture of compounds which can be fractionated. The fractions exhibit anticancer activity comparable to, or higher, than the activity of unfractionated oxidized carotenoid.
EP0994716B2 Maternal immune secretions and their use in the treatment and/or prophylaxis of conditions of the human body Medicaments formed from maternal immune secretion having biological activity characteristic of human saliva and other mucosal secretion and which is tolerated by humans can be used for the treatment and/or prophylaxis of conditions of the human body such as the buccal cavity characterised by a loss of normal mucosal or the normal biological properties thereof. The secretions are suitably egg fluid or milk from a domestic animal or replicas thereof. These secretions can be enriched with the native immunoglobulin found therein so that they have a potency which approximates that of hyperimmunised immunoglobulin. The medicaments have particular application in the treatment and/or prophylaxis of oral infection, dental caries, conditions of the buccal cavity characterised by inflammation, xerostomia and halitosis.
US20110135752 Methods For Preserving Ophthalmic Solutions and Preserved Ophthalmic Solutions A preservative system for aqueous ophthalmic solutions is provided, where the preservative system comprises a hydrogen peroxide source, at least one hydrogen peroxide stabilizer and an alkali earth metal salt.
US20130035333 Use of cinnabarinic acid as a modulator of immune responses in autoimmune disorders The present invention provides compounds and methods for preventing and treating an immune disorder in a subject.
CN101940795A Applications of DLK1 gene, siRNA (small interference Ribonucleic Acid), BM-MSCs (Bone Marrow Mesenchymal Stem Cells) and FGF2 (Fibroblast Growth Factor2) The invention discloses applications of a DLK1 gene as a target spot for curing hepatic fibrosis-renal tubular ectasia syndrome; namely the DLK1 gene is used as the target spot for designing a relevant medicine to reduce DLK1 expression and inhibit hepatic stellate cell activation so as to reduce the hepatic fibrosis-renal tubular ectasia syndrome. The invention also discloses applications of siRNA, bone marrow mesenchymal stem cells and cell factors FGF2 to preparing the medicine for curing the hepatic fibrosis-renal tubular ectasia syndrome.
CN102391346A Oleanane saponin compounds and purpose thereof The invention relates to oleanane saponin compounds aescin A and aescin B extracted and separated from aesculus carnea, and a purpose thereof. The oleanane saponin compounds have a chemical general formula as the following. The R group represents =O or -OH. As a result of experiments, the compounds has activities such as malignant tumor inhibiting, body immunity improving, liver disease preventing and curing, cardio-cerebrovascular disease preventing and curing, and diabetes mellitus preventing and curing. The invention provides novel medicine resources for treating malignant tumors, improving body immunities, and preventing and curing liver diseases, cardio-cerebrovascular diseases or diabetes mellitus.
CN1669554A Liposome vitality conazole preparation The invention relates to an externally use medicinal preparation, which mainly comprises (by weight ratio), (1) 0.08-0.8% voriconazole, (2) 10-32% phosphatides or their derivatives, (3) 0.3-10% cholestrins or their derivatives, (4) acid liquor 10-40% capable of dissolving voriconazole, phosphatides or their derivatives, cholestrins or their derivatives, (5) alkaline solution 10-40%, (6) bracket agent 1-5%.
WO2010018435A1 Amide glycosides The invention relates to the O-glucosylated amide derivatives, which are inhibitors of Sodium dependent glucose co transporter (SGLT), particularly SGLT2 and method of treating diseases, conditions and/or disorders inhibited by SGLT2 with them, and processes for preparing them.
US7390793 Have fixed, preselected hydrodynamic diameters and are formed from basic or acidic amphiphilic compounds; compound E5564 and derivatives The present invention provides micelles, solutions comprising micelles, methods for preparing micelles, and methods for delivering micelles to patients. The micelles have fixed, preselected hydrodynamic diameters and are formed from basic or acidic amphiphilic compounds.
CN103083354A Compound sodium chloride eye drops The invention discloses compound sodium chloride eye drops comprising the components of: sodium chloride, potassium chloride, sodium bicarbonate, hydroxypropylmethyl cellulose, an antiseptic of ethylparaben, and a solvent of water. According to the compound sodium chloride eye drops provided by the invention, a proper amount of hydroxypropylmethyl cellulose is used for regulating the viscosity, and ethylparaben is adopted as the antiseptic, such that the viscosity is appropriate, and a preservative effect is stable. The eye drops have properties similar to those of human body's own tear secretion. With the eye drops, moisture can be supplemented for eyes, eye surface can be moisturized, and a mucinous water-absorbent solution is formed and covered on the surface of eyes, such that eyes can be protected, and patient symptoms can be ameliorated. The eye drops can be used for effectively relieving and treating xerophthalmia.
CN101317845B Pharmaceutical use of 6-aryl substituted pyridine compounds The present invention provides application of 6-aryl-3-substituted methylene phenyl - pyridine derivative and medicinal salt to preparation of antitumor drugs. The compound has the activity of remarkably restraining growth of human poor differentiation stomach sdenocarcinoma tumor, oral epithelium tumor, liver cancer, chronic myelogonium leukaemia, oophoroma, carcinoma of uterine cervix, nasopharyngeal carcinoma, lung cancer, prostatic cancer, myelogonium leukaemia and mouse lymph oncocyte line and also has substantive broad spectrum activity. The compound can be used for preparing the antitumor drugs.
EP1765817A1 Thiazolinone unsubstituted quinolines The present invention refers to thiazolinone quinoline derivatives of the formula (I) having no substitution on the quinoline ring, and being active as CDK1 inhibitors; to processes for the manufacture of said compounds as well as the use of said compounds for the production of medicaments.
WO2007114978A3 Method for treating hiv infection through co-administration of tipranavir and pa-457 A method for treating HIV infection through co-administration of tipranavir and PA-457.
CA2803900A1 Combinations of kinase inhibitors for the treatment of cancer The present invention provides methods of treating cancer by administering a compound of formula (I), optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with an inhibitor that targets HER2 and/or HER3.
CN1651455A Pseudo portulaca oleracea saponin compound, total sapon in and its application in medicine A general pseudopurslane saponin extracted from pseudopurslane is composed of bacopaside I, bacopasaponin C, bacopasaponin D, and their mixture, which can be used to prepare the medicines for treating tumor, depression and senile dementia.
US7691844 4-(2-fluorophenylbenzoyl-4-aminobenzoyl)-3'-(2-(N,N-dimethylaminoethylaminocarbonyl))-4-aza-[6,4]-spiro-[5,6]-benzoundec-2'-ene; inner ear disorders, hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.
WO2007030537A1 Topical formulations containing o-desmethyl venlafaxine (odv) or its salts The present invention provides topical compositions comprising O-desmethylvenlafaxine (ODV), a selective serotonin and norepinephrine re-uptake inhibitor, or a pharmaceutically acceptable salt thereof. In certain embodiments, the inventive topical formulations contain one or more percutaneous/permucosal absorption enhancers. Also provided are methods of preparing and using these compositions for the treatment of various diseases or conditions such as vasomotor symptoms and pain.
WO2014095663A1 New use of aclidinium The present invention provides aclidinium or any of its steroisomers or mixture of stereoisomers, or a pharmaceutically acceptable salt or solvate thereof, for improving the physical activity in respiratory patients.
CN102240285A Amoxicillin and potassium clavulanate tablet for dogs and cats, and its preparation method and application The invention relates to an amoxicillin and potassium clavulanate tablet for dogs and cats, and its preparation method and application; the tablet is mainly used for treating and preventing infectious diseases of dogs and cats. According to the invention, the problem of control scope for environmental temperature and humidity in production of the tablet is solved, accessories that guarantee the stability of the tablet are obtained through screening, and a package form that ensures stabilization of the tablet is employed. The tablet is prepared by granulating amoxicillin in advance and then mixing amoxicillin granules with potassium clavulanate for tabletting, which guarantees the quality of tabletting on one hand and reduces the possibility of decomposition of potassium clavulanate on the other hand. The amoxicillin and potassium clavulanate tablet for dogs and cats comprises, by weight, 5 to 45% of amoxicillin, 1 to 20% of potassium clavulanate, 50 to 90% of a diluent, 1 to 10% of a disintegrating agent, 1 to 5% of an adhesive, 0.1 to 3% of a sweetener, 0.2 to 2% of an aromatic and 0.5 to 3% of a lubricant, wherein the carrier for potassium clavulanate is microcrystalline cellulose. The preparation method mainly comprises the steps of pulverizing, granulating, drying, size grading, granule mixing, tabletting and packaging.
WO2009120052A1 Pharmaceutical composition having a synergistic effect, for the treatment of high blood pressure and dyslipidemia The invention relates to a synergistic pharmaceutical composition containing an angiotensin II AT1 receptor antagonist combined with one or more statins for the treatment of high blood pressure and dyslipidemia in mammals.
CA2602464A1 Methods of treating osteoporosis and secondary hyperparathyroidism using 20-methyl, gemini vitamin d3 compounds The invention provides for methods of using 20-methyl Gemini vitamin D3 compounds to treat osteoporosis and secondary hyperparathyroidism.
WO2010058416A1 Quinazolinone linked pyrrolo[2,1 -c][1.4]benzodiazepine hybrids as potential anticancer agents and process forthe preparation thereof The present invention provides a compound of general formulae 5a-r, 9a-i to 13a-i and 17a-i to 22a-i, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1- c][1,4]benzodiazepine hybrids of general formulae 5a-r, 9a-i to 13a-i and 17a-i to 22a-i.
CN101548962A Preparation method of lutein microcapsule The invention relates to a preparation method of the lutein microcapsule with the advantages of simple operation, low costs and high purity. the preparation method comprises the following processing steps of: taking marigold flowers, adding 0.5 to 3 times amount water and 0.005 to 0.1 times amount cellulose, fermenting for 10 to 30 hours under the condition of 30 to 60 DEG C, adding 2 to 30 times amount ethanol, adjusting the PH with NaOH to be alkaline, heating reflux, filtering while hot, adjusting the PH with HCl to be neutral, decompressing and recycling the ethanol, adding the liquid into the macroporous absorption resin column, eluting impurity with water, eluting with 30 to 90% ethanol, collecting eluate, concentrating, adding hexane, methanol, and water with appropriate amount, refrigerating, completely crystallizing, separating the crystallization, washing , drying, grinding, passing 100 mesh sieve, adding modified starch, gelatin and water to make suspension, colloidal milling, and spray drying. The industrialization amplification is easily realized by using the method for preparing the lutein microcapsule.
CN101108189A Application of estrogen for preparing medicament assisting or separately treating and preventing uterine inertia type post partum bleeding disease of puerpera The invention discloses the application of estrogen for preparing drug that treats or prevents postpartum hemorrhage and uterine inertia of woman in labor. The invention discloses a new function of estrogen, that is, the estrogen can be applied in coordination with oxytocic hormone or applied independently to fast cure and prevent the postpartum hemorrhage and uterine inertia of woman in labor. Therefore, this function of the estrogen can be applied for the preparation of drug.
US8067221 Von Willebrand factor (vWF)-cleaving protease This invention is intended to isolate and identify a vWF-specific cleaving protease. The vWF-specific cleaving protease cleaves a bond between residues Tyr 842 and Met 843 of vWF and comprises a polypeptide chain having Leu-Leu-Val-Ala-Val (SEQ ID NO: 1) as a partial sequence, and more preferably comprises a polypeptide chain having the partial N-terminal amino acid sequence of a mature protein, Ala-Ala-Gly-Gly-Ile-Leu-His-Leu-Glu-Leu-Leu-Val-Ala-Val (SEQ ID NO: 2), and having a molecular weight of 105 to 160 kDa in SDS-PAGE under reducing or non-reducing conditions. Isolation and identification of this vWF-specific cleaving protease have led to the possibility of replacement therapy for patients having diseases resulting from a deficiency of the protease, such as thrombotic thrombocytopenic purpura.
WO2006088075A1 Pyridyl non-aromatic nitrogenated heterocyclic-1-carboxylate ester derivative [PROBLEMS] To provide a compound which can be used for the treatment of a disease associated with a fatty acid amide hydrolase (FAAH), particularly pollakiuria/incontinence of urine, overactive bladder and/or pain. [MEANS FOR SOLVING PROBLEMS] It is found that a novel pyridyl non-aromatic nitrogenated heterocyclic-1-carboxylate ester derivative and a pharmaceutically acceptable salt thereof have a potent FAAH inhibitory activity. The derivative is superior in increasing the effective bladder capacity and in improving pollakiuria and has an anti-allodynic effect. Therefore, this compound can be used for the treatment of pollakiuria/incontinence of urine, overactive bladder and/or pain.
CN102725292A Imidazopyridines as a novel scaffold for multi-targeted kinase inhibition Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed. Formula (I).
WO2014048547A1 Alpha hydroxy amides The present invention relates to alpha hydroxy amides including compounds of formula (I) and related compounds and their use in the prophylaxis and treatment of inflammatory disorders and diseases, wherein T1, T2, W and Rw has the meaning given in claim 1.
CN103417946A Drug for treatment of urinary calculus The invention relates to drug for the treatment of urinary calculus. The drug is made with, by weight, common Jasminorange leaf and twig, common Bur-reed rhizome, eucommia bark, rhizome of oriental water plantain, rhizome of paniculate Bolbostemma, Chinese honey locust, Szechuan lovage rhizome, tree peony bark, dried black soybean sprout, Chinese thorowax root, Psammosilene Tunicoides root, Turpinia leaf, rhizome of Chinese atractylode, Szechwan Chinaberry fruit, Himalayan mayapple fruit, Philippine violet herb, Japanese ampelopsis root, tabasheer, pummelo peel, Zaocys dhumnades, fruit of princesplume ladysthumb, sea-ear shell, leaf of paniculate microcos, dried longan pulp, common bletilla pseudobulb, Chinese wax gourd peel, humifuse euphorbia herb, scorpion, small centipeda herb, dried ginger, common coltsfoot flower, divaricate Saposhnikovia root, manyinflorescenced sweetvetch root, ophicslcite, gorgon euryale seed, longtube ground ivy herb, Chinese honeylocust spine, cockscomb flower, common lophatherum herb, Lapis Chloriti, chingma abutilon seed, rangooncreeper fruit, wild buckwheat rhizome, pine nodular branch, long pepper, oriental wormwood, stakactite, Chinese starjasmine stem, lotus leaf and common dayflower herb. The drug has the advantages that the formula of the drug is simple, the drug is cheap and has specific curative effect, and the drug is highly suitable for patients and is suitable for wide clinical popularization.
WO2008017264A1 Pharmaceutical composition comprising methyl donors or methyl donor enhancers and anti-viral compounds A pharmaceutical composition for the treatment of viral diseases comprises: 1) at least one methyl donor or methyl donor enhancer, preferably betaine or combination of betaine, folic acid and vitamin B 12, and 2) at least one anti-viral compound, preferably interferon or lamivudine. Methyl donors and methyl donor enhancers increase the anti-viral effect and therapeutic effect for treating viral diseases of anti-viral compounds.
US20110256147 Diagnostic and treatment methods for cancer based on immune inhibitors Methods of diagnosis and treatment of malignant tumors, in particular ovarian tumors, using GD3 and GD3 inhibitors. Also provided are methods of modulating the immune system of a mammal by the administration of a GD3 and GD3 inhibitors.
US20100240629 Polymorphs of fluticasone furoate and processes for preparation thereof The present invention provides crystalline forms of Fluticasone furoate, characterized by the data disclosed in the specification; pharmaceutical compositions comprising any one or combination of the crystalline forms of Fluticasone furoate and at least one pharmaceutically acceptable excipient; and the use of the crystalline forms of Fluticasone furoate in the preparation of pharmaceutical formulations.
WO2007143600A3 Sheddase inhibitors combined with cd30-binding immunotherapeutics for the treatment of cd30 positive diseases The present invention is directed to pharmaceutical methods for the treatment of CD30 positive diseases, such as Hodgkin's disease, by administration of a combination of at least one sheddase inhibitor and at least one anti-CD30 immunotherapeutic.
CN103463140A Disinfection repairing liquid The invention discloses disinfection repairing liquid which is characterized by consisting of the following components in percentage by mass: 10% of chlorhexidine gluconate, 20% of chlorella biological-activity substance and 70% of pure water, or consisting of 10% of chlorhexidine gluconate, 30% of chlorella biological-activity substance and 60% of pure water, or consisting of 1% of chlorhexidine gluconate, 20% of chlorella biological-activity substance and 79% of pure water. The disinfection repairing liquid is prepared by the steps of pouring the chlorhexidine gluconate of the formula amount and the pure water of 2/3 of the formula amount into a mixing container, and sufficiently and uniformly stirring; putting in the chlorella biological-activity substance, and shaking while uniformly stirring; finally adding the pure water of 1/3 of the formula amount to obtain a finished product. The disinfection repairing liquid disclosed by the invention has a good curative effect on gynecological diseases such as vaginitis, uterine fibroid and the like; the disinfection repairing liquid is directly sprayed onto the wound caused by scalding or diabetes to avoid further infection caused by binding and reduce the generation of scar tissues; the disinfection liquid thoroughly kills staphylococcus aureus, pseudomonas aeruginosa, escherichia coli, candida albicans and aspergillus niger within 1 minute, is suitable for the disinfection of a pre-operation wound, and can effectively promote the skin wound healing to relieve the itch and pain.
CA2566655C Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them The present invention relates to pharmaceutical formulations comprising at least one acid-labile proton pump inhibiting agent and at least one antacid, which have improved bioavailability, chemical stability, physical stability, dissolution profiles, disintegration times, safety, as well as other improved pharmacokinetic, pharmacodynamic, chemical and/or physical properties. The present invention is directed to methods, kits, combinations, and compositions for treating, preventing or reducing the risk of developing a gastrointestinal disorder or disease, or the symptoms associated with, or related to, a gastrointestinal disorder or disease in a subject in need thereof.
CN103417772A Gynecological preoperative bowl preparation oral drug The invention discloses gynecological preoperative bowl preparation oral drug and solves the problems in gynecological preoperative treatment. The drug is characterized by being made with, by weight, 10-30 parts of horseweed herb, 6-12 parts of cinnamon seeds, 3-10 parts of Chinese mosla, 6-12 parts of Chinese starjasmine stem, 3-10 parts of loofah sponge, 6-12 parts of Barbary wolfberry fruit, 6-12 parts of Dipsacus root, 6-12 parts of grassleaf sweelflag rhizome, 6-12 parts of sunflower flower, 1-5 parts of Turbo cornutus solander, 3-10 parts of ox horn bone, and 10-25 parts of magnesium sulfate. Clinical experiments show that the gynecological preoperative bowl preparation oral drug has good effect of gynecological preoperative bowel cleansing, and is worthy of clinical application and popularization.
US7314955 Crystalline form "C"; amidating D-phenylalanine methyl ester hydrocholoride with trans-4-isopropylcyclohexane carboxylic acid in a halogenated hydrocarbon; hydrolyzing to form free acid The present invention relates to a novel crystalline form of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine and methods for preparing the same.
WO2013018735A1 Amidine compound or salt thereof The purpose of the present invention is to provide a novel compound which has an anti-fungal activity on pathogenic fungi including fungi belonging to the genus Candida, the genus Aspergillus and the genus Trichophyton and is useful as a medicinal agent. A compound represented by formula (I) (wherein A1 represents a nitrogen atom or a group represented by formula CR6; A2 and A3 are the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; R1 represents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; R2 and R3 are the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group or a C1-6 alkoxy group; and R4 and R5 are the same as or different from each other and independently represent a hydrogen atom, a C1-6 haloalkyl group, a C1-6 alkyl group or the like) or a salt thereof is useful as an anti-fungal agent.
EP1056459B1 Treatment of hiv infections Disclosed is a method of treating an HIV-infected host including administering to the host a therapeutic agent that is cytotoxic or cytostatic with respect to CD4+ T cells, but has reduced cytotoxic or cytostatic activity with respect to T lymphocyte stem cells, in a CD4+ T cell cytotoxic or cytostatic effective amount. Also disclosed is a method of treating an HIV-infected host including administering highly active antiretroviral therapy; and coadministering to the host a therapeutic agent that is cytotoxic or cytostatic with respect to CD4+ T cells, but has reduced cytotoxic or cytostatic activity with respect to T lymphocyte stem cells, in a CD4+ T cell cytotoxic or cytostatic effective amount. Also disclosed is a method of ex vivo or in vitro treatment of blood derived cells, bone marrow transplants, or other organ transplants including treating the blood derived cells, bone marrow transplants, or other organ transplants with a therapeutic agent that is cytotoxic or cytostatic with respect to CD4+ T cells, but has reduced cytotoxic or cytostatic activity with respect to T lymphocyte stem cells in a CD4+ T cell cytotoxic or cytostatic effective amount. Kits and compositions useful in the practice of the invention are also disclosed.
WO2009037719A1 Novel compounds as dipeptidyl peptidase iv (dpp iv) inhibitors The present invention is related to novel compounds of the general formula (A), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors, which are useful in the treatment or prevention of diseases particularly Type II diabetes, other complications related to diabetes and other pathogenic conditions in which DPP IV enzyme is involved.
CN102988433A Pharmaceutical composition for treating pneumonia, and preparation method thereof The invention provides a pharmaceutical composition for treating pneumonia, which is prepared by taking amoxicillin, prednisone tablets, chlortrimeton tablets, aminophylline tablets, vitamin C tablets and radix isatidis tablets as raw materials. The invention also provides a preparation method and usage of the pharmaceutical composition. The medicine has better effects in the aspects of relieving clinical symptoms such as fever, cough and the like caused by pneumonia, controlling inflammation, improving ventilation function and the like, achieves the aims of comprehensively treating the pneumonia, and has the characteristics of being convenient to take, low in cost, good in treatment effect, safe in medication, etc.
US20060100269 Use of 10-aminoaliphatyl-dibenz[b,f]oxepines for the treatment of degenerative ocular disorders The present invention relates to novel uses of 10-aminoaliphatyl-dibenz[b,f]oxepines for the treatment of degenerative ocular disorders.
WO2008155651A3 Inositol for induction of ovulation A composition comprising inositol for induction of ovulation in a subject by administering to the subject the composition in such a quantity so as to provide at least 2 g/day of inositol.
US20130065836 Biomarker for gastric cancer The present invention provides a method for diagnosing and determining prognosis of gastric cancer in a subject by detecting suppressed expression of the BCL6B gene, which in some cases is due to elevated methylation level in the genomic sequence of this gene. A kit and device useful for such a method are also provided. In addition, the present invention provides a method for treating gastric cancer by increasing BCL6B gene expression or activity.
US7501455 For parental injection of water insoluble drugs such as paclitaxel, propofol, amphotericin B, camptothecin, gemfibrozil and cyclosporin A; plasma protein such as serum albumin, an immunoglobulin, a glycoprotein, an interferon, or an interleukin, in controlled aggregation state The invention is related to water-soluble products and pharmaceutical formulations in solid or liquid form mainly for parenteral use. They consist of or comprise a therapeutically active substance (having low aqueous solubility and a substantial binding affinity to plasma proteins) and a plasma protein fraction in controlled aggregation state, whereby the said active substance and the said protein fraction are bound to each other by way of non-covalent bonds. It also covers processes for the preparation of the product and pharmaceutical formulation by dissolving the water-insoluble active substance in a water-miscible, pharmaceutically acceptable solvent, combining said solution with the aqueous solution of a plasma protein fraction in controlled aggregation state whereby a true solution is obtained containing the said active substance and the said protein fraction bound together by way of non-covalent bonds. Optionally a further pharmaceutically acceptable auxiliary additive—such as a protein aggregation controller and/or a stabilizer—may be present. The organic solvent is eliminated by dialyzing, ultrafiltrating, diafiltrating and/or lyophilising. The solid products consisting of the active substance and the protein are also protected. On optional dissolution in water clear, liquid compositions are obtained suitable for direct parenteral or other administration. Method of treatment is also covered. A series of water-insoluble substances is enlisted with appropriate protein fractions to be used.
WO2006068041A1 Composition having effect of promoting the decomposition of body fat and food or food additive containing the same It is intended to provide a composition having an effect of promoting the decomposition of body fat and a food or a food additive containing the same. By orally taking a composition (1) containing, as the main component, ceramide (2) extracted from a plant, a fungus, a yeast, a mushroom, an animal, a marine animal or an insect (for example, rice bran, konjak, wheat, corn, bovine brain, etc.) and a food or a food additive containing the same, the production of fat and sugar in the body can be promoted. This composition (1) elevates the expression amount of a thyroid hormone receptor β (5) gene on the surface of a target cell (4) and thus promotes the decomposition of fat. Also, it elevates the expression amount of a carnitine acetyltransferase (15), which is an enzyme participating in the β oxidation (13) lipid metabolism, gene and thus promotes the fat and sugar energy production in the target cell (4). Namely, the oral intake of the food and/or the food additive containing ceramide (2) contributes to the reduction in body weight and body fat, i.e., exerting a so-called diet effect.
CN103505417A 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride aerosol and preparation method thereof The invention discloses a 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride aerosol and a preparation method thereof. A 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride aerosol formula contains the following components by weight: 0.05-20% of 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride, 0-20% of co-solvent, 0-2% of surfactant, and 60-99.95% of propellent. A preparation method contains the following steps of: according to the formula, uniformly mixing the 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride, the co-solvent and the surfactant, adding a mixture into an aerosol enclosed container, and then pressing the propellent in, to complete the preparation. The 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-1-acetoxime hydrochloride aerosol has good bioavailability.
US20100099763 Triterpene compounds which are effective on improvement of brain function The present invention relates to the triterpene compounds improving in brain functions. In particular, the present invention relates to a novel use of the triterpene compounds represented by the Formula 1 for improving decreased memory and a pharmaceutical composition for improving brain functions comprising the triterpene compounds represented by the Formula 1.
US20090123545 Rapid Onset and Short Term Modafinil Compositions and Methods of Use Thereof Compositions are described that comprise a modafÊnil component that is a combination of the d- and l-enantiomers of modafinil and wherein the modafÊnil component is greater than 50% by weight d-modafÊnil for use in promoting or enhancing the state of wakefulness, alertness, and/or central nervous system stimulation in an individual.
WO2013091507A1 Heterocycle amido alkyloxy substituted quinazoline derivative and use thereof A heterocycle amido alkyloxy substituted quinazoline derivative as represented by the structure (I) and pharmaceutically acceptable salt thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family.
US20080125491 screening for neuroprotectants such as -Isobutyryl-1,4-a-dimethyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-1-carboxylic acid amide, used for the prevention of neurodegenerative diseases and cardiovascular disorders The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In certain embodiments, the GPCR is human. In certain embodiments, the GPCR is expressed endogenously by neuronal cells or muscle cells. In certain embodiments, the GPCR is neuroprotective or myoprotective. In certain embodiments, the GPCR is a Humanin receptor. The present invention also relates to methods of using a modulator of said GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of neurodegenerative diseases in general, including Alzheimer's disease, Parkinson's disease, prion-associated disease, stroke and motor-neuron disease in particular, peripheral neuropathy, cerebral amyloid beta-protein angiopathy, and ischemic heart disease, including myocardial infarction and congestive heart failure.
CN1732947A Antibacterial medicinal composition of cefsulodine sodium for injection Disclosed is an antibacterial medicinal composition of cefsulodine sodium for injection, which comprises cefsulodine sodium and amoxicillin sodium by the weight ratio of 1-32 : 1. The composition can be used for treating various infection caused by sensitive bacteria.
WO2006073367A1 5-thioxo-1,5-dihydro-2h-pyrrol-2-one derivatives as liver x receptor modulators The present invention relates to certain novel compounds of the Formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer´s disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
CN1562041A Alpostadil freeze-dried emulsion and its preparing method A freeze-dried emulsion of prostaglandin E1 is prepared from prostaglandin E1, the oil for injection, stabilizer, emulsifier, pH regulator, freeze-drying protector and the waer for injection. Its preparing process is also disclosed.
US20080176833 Dihydropyridine derivatives as useful as protein kinase inhibitors This invention provides novel dihydropyridine derivatives of the formula I having protein tyrosine kinase inhibitory activity, to process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions.
CA2649360A1 Mono and di-substituted oxycodone compounds and compositions The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to oxycodone in a manner that substantially decreases the potential for overdose. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of oxycodone and may also provide sustained release characteristics and/or reduced side-effects. Further the compounds and compositions of the invention are useful in preventing addiction and susceptibility to addiction of oxycodone.
WO2005107872A3 Treating respiratory diseases with gycopyrrolate and analogues Glycopyrrate or an analogue thereof is useful for the treatment of bronchospasm or as a rescue medication.
CN102370650A Compound triamcinolone acetate-urea cream and preparation method thereof The invention discloses compound triamcinolone acetate urea-cream and a preparation method thereof, relating to the technical field of medicine. The compound triamcinolone acetate-urea cream consists of triamcinolone acetate, urea and an emulsion substrate. In the compound triamcinolone acetate-urea cream, triamcinolone acetate serves as a medium-efficiency glucocorticoid which can be used for eliminating fever, flushing and swelling caused by local non-infectious inflammation; and urea has the effects of dissolving and denaturalizing keratoprotein and enhancing the cuticle layer hydration, so that skin is softened, and cracking is prevented. The compound triamcinolone acetate urea-cream has the effects of suppressing movement of inflammatory cells to inflammatory positions, preventing inflammatory media from being released, stability a lysosome membrane, suppressing immune reactions and improving the stress ability of a mechanism to noxious stimulus.
EP1200395B1 Urea derivatives as inhibitors of ccr-3 receptor Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.
US20100035915 Indolizine derivatives and the use thereof as antidiabetics Novel compounds of the formula (I), in which X, Y, R, R1, R1, R1′, R2, R2′, R3, R4, R4′, R5 and n have the meanings indicated in patent claim 1, are suitable as antidiabetics.
US20120115821 Composition and method for treating skin conditions Compositions and methods for treatment of conditions affecting skin and/or mucosal surfaces of a subject that make use of an imidazoquinoline compound and a retinoid agent are described.
WO2010142143A1 Pirfenidone compound, preparation method and use thereof A kind of modified compound of pirfenidone, its preparation method and use for preparing the drug for anti-organ or tissue fibrosis is disclosed.
US20080171089 Stable anti-nausea oral spray formulations and methods Stable formulations of selective 5-hydroxytryptamine receptor antagonists for oral spray administration for absorption by the oral mucosa and related methods of preparation and administration are provided. A preferred embodiment includes ondansetron in a concentration of about 5.1 to about 5.2% w/w; propylene glycol in a concentration of about 60.1 to about 60.3% w/w; water in a concentration of about 5.3 to about 5.4% w/w; and ethanol in a concentration of about 27.1 to about 27.3% w/w. Additional preferred embodiments are preservative free and/or non-aqueous or primarily non-aqueous.
WO2008012110A3 Annellated pyrrole compounds for cancer management The present invention relates to the use of annellated pyrrole compounds and in particular ML3000 (licofelone), salts or derivatives thereof, for cancer management, and in general to the use of a compound of Formula (I): wherein the variables have the meanings given in the present description, for the prevention and/or treatment of neoplasia, in particular neoplasia selected from the group consisting of papilloma, carcinoma, adenoma and adenocarcinoma, e. g. human airway or colorectal carcinoma, preferably fast-growing, multidrug resistant and/or COX-2 negative neoplasia. The invention further relates to pharmaceutical compositions for the aforesaid purposes, comprising annellated pyrrole compounds and in particular ML3000 (licofelone), optical isomers, salts or derivatives thereof, as well as to a method of treating and/or preventing neoplasia and/or restoring the ability to undergo apoptosis in a cell having lost the same. This treatment ameliorates, diminishes, actively treats, reverses or prevents any disease related to insufficient apoptosis, in particular neoplasia, and it may be combined with irradiation, heating and treatment with a cytotoxic agent for preventive and/or curative purposes.
CA2389650C Composition for treatment of constipation and irritable bowel syndrome Constipation and Irritable Bowel Syndrome are treated by a delayed and sustained release composition of an opioid antagonist which commences release of the opioid antagonist in the mid to distal small intestine or ascending colon and provides sustained release along any remaining part of the small intestine and along the colon. Preferred opioid antagonists are naloxone and naltrexone.
US20120064155 Oral pharmaceutical composition for use in respiratory diseases A modified-release oral pharmaceutical composition in capsules with microspheres contains loratadine, phenylephrine and pharmaceutically acceptable excipients. The composition has immediate bioavailability, with plasmatic concentration values within the therapeutic window with a uniform, continuous release. A method for the production of the composition and a method for treatment as a nasal decongestant and an antihistamine are included.
CN101437503A Compositions to reduce blood glucose levels and treat diabetes The invention discloses compositions that effectively reduce and stabilize glucose levels in the blood of mammals, specifically in pre-diabetic patients and patients with type 2 diabetes mellitus (T2DM). Composition 1 (Comp1) reinforces efficacy of Mg salt to reduce glucose level by the combination of Mg salt with anti-inflammatory agents konjac-glucomannan (KGM), vitamin C and alpha-lipoic acid (a-LA). Composition 2 (Comp2) provides safety for chromium picolinate (CrPic) by the combination of CrPic with anti-inflammatory agents KGM, vitamin C and a-LA that inhibits oxygen radicals. Compositions may optionally include cinnamon extract (CE) or another insulinogenic nutraceutical agent, American ginseng (AG), Uncaria tomentosa, Uncaria guianensis and Urtica dioica.
CA2662617A1 Quinazoline based egfr inhibitors containing a zinc binding moiety The present invention relates to quinazoline containing zinc-binding moiety based derivatives that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
US6884433 Time release agents comprising drugs such as tacrolimus in solid solutions Sustained release formulation containing tacrolimus or its hydrate is provided. The time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours. The time is measured in accordance to the Japanes Pharmacopocia, the 13-th edition, Dissolution Test, No. 2 (Puddles method, 50 rpm) using an aqueous 0.005% hydroxypropyl cellulose solution. This aqueous test solution is adjusted to pH 4.5, accordingly. The formulation further comprises a solid base which is a water-soluble or water-insoluble polymer. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. The formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune disease. In addition, a solid dispersion composition is provided. The solid dispersion comprises tacrolimus or its hydrate in a mixture containing water-soluble or water-insoluble polymer and an excipient.
WO2009075677A1 O-desmethyl-venlafaxine for treating major depressive disorder The present invention provides methods for treating MDD. In general, the methods comprise administering to a patient in need thereof a daily dose of about 50 mg ODV or an equivalent amount of a pharmaceutically acceptable salt thereof. In certain embodiments, a patient in need of treatment is characterized by a primary diagnosis of MDD. In some embodiments, the dose is administered as a single daily dose. In one set of embodiments, the methods involve administering an oral dosage form comprising the succinate salt of ODV.
US20120052132 Compositions and methods for treatment of body weight conditions A nutritional supplement composition having therapeutically effective amounts of milk minerals including calcium, a protein source including kappa-casein fragment 106-169, and enzyme-inhibiting peptides is provided for the treatment of body weight conditions. The nutritional supplement composition is administered in amounts effective for limiting weight gain and/or enhancing weight loss, as well as promoting overall good health, in the treatment of body weight conditions, including overweight and obesity.
EP1089727B1 Liposomal formulations of busulphan Pharmaceutically acceptable liposome-encapsulated busulphan formulations for parenteral administration are provided, as well as a process for their manufacture. The formulations are stable, have improved biodistribution and significantly reduced side effects over those produced by oral administration or parenteral administration of free drug. The formulations are useful as part of bone marrow transplant conditioning regimens.
US20130053446 Pharmaceutical preparations having individualized dosage and structure A manufacturing device capable of creating individualized dosages of pharmaceutical preparations in which a metering system and a means of performing non-destructive chemical analysis of individual manufactured units are controlled by a microprocessor to precisely control the content and structure of each individual unit.
CN101564400A Antibacterial supermolecule aquogel and preparation method and application thereof The invention discloses a method for in-situ preparing antibacterial supermolecule aquogel. The method comprises the following operation steps: silver nitrate crystal and polyethyleneglycol-polypropylene glycol-polyethyleneglycol triblock copolymer solution are mixed and stirred to obtain mixed solution; the steps of stirring the mixed solution for 15 minutes and ultrasonically dispersing the mixed solution for 5 minutes are alternatively carried out for 2-4 hours to obtain nano silver sol; and the nano silver sol and Alpha-cyclodextrin solution are mixed, stirred and stands at the room temperature to obtain hydrogel. The hydrogel can be used for preparing injectable drug carriers. The invention has the advantages of simple operation, adjustable gel strength and the gelation time, room temperature forming, no involvement of chemical cross linking reaction and the usage of organic solvent, favorable biocompatibility and antibacterial property of obtained gel, and the like and is prospective to be widely applied in the field of biomedical engineering materials.
CN101199539B Application of locust glycolipid in preparing anti-skin ringworm medicament The invention discloses an application of sophorolipids in preparing drugs for resisting dermatophyte, and an application of a combination where the sophorolipids is used as an effective component inpreparing drugs for resisting dermatophyte. With low price, little dosage and remarkable antibacterial effect, the invention has no side effect on the human, and in certain aspects can be used as a drug for replacing conventional antifungal drugs which produce heat resistance easily and drugs for treating skin tinea disease such as corticosteroid with severe side effects. Thus, the invention has great application prospect.
WO2006116151A1 Benzofuranyl alkanamine derivatives and uses thereof as 5-ht2c agonists Compounds of formula I pr pharmaceutically acceptable salts thereof are provided: wherein each of R1, R1’ , R2, R3, R4, n, and Ar are as defined in the description which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
WO2010056585A3 Heteroaryl diamide compounds useful as mmp-13 inhibitors Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).
US20100069470 Identification of protein biomarkers associated with lymph node metastasis in colorectal cancer Disclosed herein are compositions and methods relating to the diagnosis, prognosis, and treatment of colorectal cancer. The compositions and methods generally relate to the differential expression of transgelin in colorectal cancer cells with metastatic potential.
CA2581493A1 Taste-masking pharmaceutical compositions The present invention relates to a pharmaceutical composition for oral administration suitable for the preparation of a ready-to-use suspension comprising coated particles comprising an active substance having an unpleasant and/or bitter taste, such as clarithromycin, and a suspension base comprising an osmotically active substance capable of providing a high osmolality to the admixture of the suspension base with an aqueous suspending medium in the ready-to-use suspension. Said ready-to-use suspension maintains its palatability over a prolonged period of time by those defined osmotic conditions.
US20130071438 Compositions and methods for the treatment of hyperplasia In accordance with the present invention, there are provided methods for treating hyperplasia in a subject in need thereof. In another aspect of the invention, there are provided methods for reducing neointimal hyperplasia associated with vascular interventional procedures. Formulations contemplated for use herein comprise proteins and at least one pharmaceutically active agent.
WO2011049093A1 Film-coated tablet which is suppressed in discoloration and odor Disclosed is a tablet containing tranexamic acid, ascorbic acid and L-cysteine, which has excellent stability and is suppressed in discoloration and unpleasant odor. Specifically disclosed is a film-coated tablet that is obtained by providing a tablet, which contains tranexamic acid, ascorbic acid and L-cysteine, with a coating film that contains a polyvinyl alcohol copolymer.
WO2005120475A3 Pharmaceutical composition for the treatment of bacterial infections and sepsis The invention relates to a pharmaceutical composition comprising at least one glycogen synthase kinase 3β(GSK-3β) inhibitor, at least one Rho-kinase inhibitor, and an optional adequate pharmaceutical carrier for producing a medicament used for the preventive or therapeutic treatment of bacterial infectious diseases including sepsis by synergistically increasing synthesis and secretion of type IIA secretory phospholipase A2 (sPLA2-IIA) into the bloodstream so as to boost the body's inherent resistance to infections. The invention relates to the field of medicine, particularly the prevention and therapy of bacterial infectious diseases, especially infectious diseases caused by Staphylococcus aureus and Escherichia coli, including sepsis. Using the inventive pharmaceutical composition or the inventive combination provides the body with efficient resistance against bacterial pathogens, above all Escherichia coli and Staphylococcus aureus by inducing optimal synthesis and secretion of secretory phospholipase A2-IIA (sPLA2-IIA) into the bloodstream. The combination of substances which block different signal transduction paths has synergistic effects, allowing for substantially greater stimulation of sPLA2-IIA synthesis and secretion while keeping the concentrations of administered substances lower than if the individual substances were used, thus reducing the risk of potential side effects in a correspondingly advantageous manner.
EP2187743A2 Formulations for treatment of ocular diseases or conditions Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium; nondispersed mass-forming liquid formulations which form a gel or gel-like substance in an aqueous medium; liquid formulations, comprising a therapeutic agent and polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including via intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration, or wet age- related macular degeneration.
US7977369 Via 3-hydroxymethyl-5-aziridinyl-1-1-methyl-2-(1H-indole-4,7-dione )propenol Methods for treating bladder cancer comprising intravesicular administration of a stabilized pharmaceutical formulation comprising 5-(1-aziridinyl)-3-(hydroxymethyl)-2-[(E)-3-hydroxyprop-1-enyl]-1-methyl-1H-indole-4,7-dione (EO9). More specifically, the stabilized pharmaceutical formulation is instilled in the bladder for a time sufficient to treat the cancer.
US20110009464 Immune system stimulation by light therapy induced apoptotic cell death in abnormal tissue The efficacy of light activated therapy treatment is enhanced by stimulating the immune system of the patient substantially above the pre-therapy level. Abnormal tissue that is destroyed by the light activated therapy releases factors that stimulate the immune system, leading to systemic reductions in abnormal tissue (i.e., reduction beyond the area treated using light), so long as the light therapy conditions favor apoptosis over necrosis. The volume of abnormal tissue destroyed is maximized to the extent possible, reducing tumor load, which reduces an amount of immunosuppressive factors in the body, enabling stimulation of the immune system to be successful.
EP2321286B1 Substituted n-oxide pyrazine derivatives A N-oxide pyrazine derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: (I) wherein: R1 represents a 4-pyridine ring, a halogen atom; R2 represents a hydrogen atom; R3 represents a hydrogen atom; R4 represents: a phenylCi-3alkyl group, this group being optionally substituted; R5 represents a hydrogen atom; in the form of a free base or of an addition salt with an acid. Use in Therapy
CN101269033A Ambroxol hydrochloride sustained-release dropping pill and preparation method thereof The invention relates to a sustained-release drug used for treating bronchitis, asthma and lung diseases as well as the preparation method thereof, and aims to supplement the deficiencies that existing tablets, capsules and oral formulations have short acting time, unsteady plasma concentration and deficient preparation method and provide a sustained-release ambroxol hydrochloride dropping pill which has good substance dispersion state, long acting time and high bioavailability. The sustained-release ambroxol hydrochloride dropping pill is prepared by adopting ambroxol hydrochloride as the ingredient, adding in hydrophilic frame ingredients and hydrophobic frame ingredients as the stroma according to a definite proportion and mixing well, heating the mixture to meltdown and mixing well, putting the melted mixture into a dropping pill machine and trickling the melted mixture into a condensing agent to be cooled off.
CN1559407A Self-micro emulsion solft capsule of dihydropyridine type calcium ion agonist, and its prepn. method A self-microemulsified softcapsule of nimodipine or nitrendipine is prepared from nimodipine or nitrendipine, coemulsifier, self emulsifier, oil and antioxidizing agent through proportionally mixing nimodipine or nitrendipine, coemulsifier and self emulsifier, constant-temp oscillating, adding oil and antioxidizing agent, stirring, cooling, and shaping.
US20050180982 Assessing metastatic potential of carcinoma cells by contacting cells in tissue sample suspected of containing carcinoma with detectable indicator capable of binding to cad-11 or cad-11 mRNA and determining presence or absence of cad-11 expression in tissue; method of preventing or terminating pregnancy A method of modulating differentiation or neoplastic transformation of cells is provided in which the cells are caused to increase or decrease cad-11 expression or function. Such method has application in affecting differentiation or neoplastic transformation of cells, preventing or terminating pregnancy by altering cad-11 function or expression in trophoblast cells, or for reducing the viability of carcinoma cells having a low to moderate metastatic potential. The use of agents which increase or decrease cad-11 expression or function is also provided, including such use for preparation of medicaments for modulating differentiation or neoplastic transformation of cells. A method for assessing the metastatic potential of carcinoma cells is also provided.
EP0941083B1 Pharmaceutical compositions containing 3-iodo-1,2-propanediol having mucolytic activity The present invention relates to pharmaceutical compositions containing 3-iodo-1,2-propanediol which are effective in increasing the output of thin respiratory tract fluid and liquefying tenacious mucus in the bronchial tree.
WO2014004054A1 Compositions and methods for treating cancer with aberrant lipogenic signaling The technology described herein relates to pinacolyl boronate substituted stilbenes for the treatment of cancers, e.g. cancers expressing abnormally high levels of SREBP1.
US20080214588 replication inhibitors; show improved ability to inhibit the replication of mutant strains, in particular strains which show double or multiple mutations in the viral genome encoding for reverse transcriptase HIV replication inhibitors of formula (I) pharmaceutically acceptable addition salts; or stereochemically isomeric forms thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
CN101229132B Nimodipine pulse sustained release mircopill preparation and preparing method thereof The invention relates to a pulsed sustained-release pellet comprising nimodipine and a preparation method is also provided. The sustained-release pellet comprises: one of gastric-dissolved and medicines containing sustained-release pellets and enteric-coated and medicines containing sustained-release pellets, or the combination. The preparation method is that: making medicines containing pellets using nimodipine and excipents, coating the medicines containing pellets with the gastric coating or the enteric coating, mixing the sustained-release pellets coated with gastric coating and enteric coating in proportion and putting the sustained-release pellets into capsules or tabletting. The pulsed sustained-release pellet of the invention has a special release behavior and needs to be taken only once per day. The release curve agrees well with the disease circadian rhythm of cerebrovascular disease patients, playing a role of the best prevention and treatment.
US8206711 Treatment of chronic lymphocytic leukemia using anti-CD20 antibodies Chronic Lymphocytic Leukemia (CLL) may be treated with antibodies directed against the CD20 antigen.
WO2012047733A2 Treatment of acne by conditioned media Disclosed are methods and compositions for treatment of acne or acneform conditions, particularly but not limited to, acne vulgaris with products generated from culture of stem or progenitor cells. Specifically, compositions of matter are disclosed which are useful for the treatment of acne and acne associated disease states, in particular acne vulgaris, by topical administration of products derived from stem cells or progenitor cells.
EP2646000A1 Chemoembolization composition comprising anti-angiogenic agents The invention relates to chemoembolization composition for anti-angiogenic agent delivery. The invention further relates to a method of preparing chemoembolization composition and to the use of chemoembolization composition in the method for treating solid tumour cancers.
US20110136877 2-phenyl phenoxyacetic acids useful for treating inflammatory disorders The present invention provides novel phenoxyacetic acids useful for the prevention and treatment of inflammatory disorders, including those affecting the respiratory system and skin. The compounds are of the general formula (I):
CN102993201A 6-(4-hydroxyl-phenyl)-3-styryl-1H-pyrazole[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitor The invention relates to a pyrazole[3,4-b]pyridine compound in a formula I. In the formula I, R1, R2, R3, R4 and R5 are defined as the specification. The compound in the formula I is a kinase inhibitor which is used for the treatment of diseases related to diabetes and diabetic complications, such as diabetic nephropathy (DN), diabetic neuropathy and diabetic retinopathy (DR). The invention also relates to the application of the compound in the formula I. The compound in the formula I is used as an active ingredient of a medicine and a pharmaceutical composition containing the compound in the formula I.
CN102510758A Lactase preparation Disclosed is a lactase preparation which does not undergo the deactivation of lactase even when the preparation is ingested prior to the ingestion of a lactose-containing food or beverage such as a milk product and therefore can decompose lactose stably and which can prevent the symptoms of lactose tolerance. Specifically disclosed is a lactase preparation comprising lactase and at least one component selected from trisodium citrate, potassium sodium tartrate, calcium carbonate, sodium carbonate and calcium hydrogen phosphate which acts as an antacid. The lactase preparation is characterized by being intended to be ingested prior to the ingestion of a lactose-containing food or beverage to decompose lactose. In the lactose preparation, the antacid is contained at such a content per unit dosage form that the pH value in the stomach can be increased to 4 or higher after the ingestion of the preparation.
US20070259827 Compositions and methods for enhancing discriminatory RNA interference The present invention provides methods for enhancing discriminatory RNA silencing by RNA silencing agents. In particular, the invention provides methods for generating RNA silencing agents which can discriminate between target and non-target mRNAs that differ in sequence by only one nucleotide. Also provided are improved RNA silencing agents with enhanced discriminatory RNA silencing, e.g., single nucleotide discriminatory RNA silencing. The compositions and methods of the invention are useful in therapeutic strategies for treating genetic disorders associated with dominant, gain-of-function gene mutations.
US20130012443 Methods of treatment of central nervous system hemorrhage using protoporphyrin ix-fe compounds Described herein are methods and compositions relating to treatment of tissue damage resulting from a central nervous system (CNS) hemorrhage with a protoporphyrin IX-Fe compound.
CN101400333A Skin-whitening agent for external application to the skin, and method for whitening the skin Disclosed is a skin-whitening agent for external application to the skin, which comprises sucrose linoleate as an active ingredient.
CN101703499A Two chemical anti-tumor drugs The invention relates to chemical anti-tumor drugs, which takes two methoxy flavonoid derivates 5,7-dyhydroxy-8-(1,1- allyldimethyl amille)-3,3',4'-trimcthoxy flavone or 5,7-dyhydoxy-8-(1,1- allyldimethyl amille)-3,4'-dimethoxy flavone as effective components. Pharmacologic test effect proves that the cell toxicity test result of the two methoxy flavonoid derivates on 31 tumor cell lines shows broad-spectrum anti-tumor effect; the model test of human tumor transplanted to nude mice is used and has strong effect for inhibiting tumor growth on human prostate cancer cells, human lung carcinoma, human colorectal cancer cells and human breast cancer cells. Pharmacokinetics tests also show that the two methoxy flavonoid derivates can be kept at a certain concentration in mice and is in favor of anti-tumor effect. Acute toxicity tests on mice show no toxicity. Therefore, the two methoxy flavonoid derivates are a broad-spectrum anti-tumor new drug with bright development prospect.
US20100234293 Novel Neurotrophic Factors The invention relates to neublastinneurotrophic factor polypeptides, nucleic acids encoding neublastin polypeptides, and antibodies that bind specifically to neublastin polypeptides, as well as methods of making and methods of using the same.
US7429596 Oxidoreductase inhibitors; anticancer agents; antiinflammatory agents This invention generally relates to pyrazolo pyrimidine derivatives useful as inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. The invention further relates to pharmaceutical compositions and methods of preventing or treating disease with 1H-Pyrrolo[2.3-d]pyrimidine derivatives. More specifically, the invention relates to a 1H-Pyrrolo[2.3-d]pyrimidine which is a compound of Formula I or II: or a pharmaceutically-acceptable salt or prodrug thereof; wherein: Y is N or CR5; Z is NR3R4, halo, H, OH, alkyl, alkyloxy, or haloalkyl; and R1a is indolyl, thiazolyl, benzyl, biphenylyl, thiophenyl, pyrrolyl, or phenyl, wherein said phenyl is substituted with at least one of OH, —NR3R4, —C(═O)NR6R7, —CN, NO2—C(═O)OH, —C(═O)O-alkyl, (C1-C4)alkyl, halo, haloalkyl or haloaryl; and wherein said indolyl, thiazolyl, benzyl, biphenylyl, thiophenyl, or pyrrolyl is optionally substituted with OH, —NR3R4, —C(═O)NR6R7, —CN, NO2, —C(═O)O—R3, (C1-C4)alkyl, halo, haloalkyl or haloaryl.
US20120128695 Teneurin c-terminal associated peptides (tcap) and methods and uses thereof The invention provides a novel family of biologically active neuropeptides and the nucleic aid molecules coding for same. The peptides are derived for the C-terminus of the teneurin family peptides (Ten M1-4). These novel peptides, referred to as teneurin C-terminal associated peptides (TCAPs) are active in neuronal communication and are implicated in a number of neuropathologies. They are particularly useful in modulating stress responses and anxiety and in the treatment of cancer.
CN101766625A Application of Morphine as medicament for promoting growth of nerve cells The invention relates to a new medical application of Morphine, in particular to an application of Morphine as a medicament for promoting the growth of nerve cells. Through a thiazolyl blue (MTT) method, the Morphine is found to be capable of promoting the growth of adrenal gland chromaffin tumor cells (PC12 cells) of rats. The Morphine has the activity of promoting the proliferation of nerve cells and can inhibit nerve cell injuries caused by a Parkinson toxic substance MPP+(1-Methyl-4-Phenylpyridiniumion). Proved by a protein immunoblotting method, the Morphine can induce the expression level of thioredoxin in the PC12 cells, thus the Morphine for protecting the nerve cells from injuries of MPP+ toxicity is related to the induction of the expression of the thioredoxin.
US20120077759 3-3-Di-Substituted-Oxindoles as Inhibitors of Translation Initiation Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.
CN102579425A Caulis Spatholobi extract, application thereof and new application of isoliquiritigenin The invention provides Caulis Spatholobi extract, an application thereof and a new application of isoliquiritigenin, and particularly provides Caulis Spatholobi extract containing isoliquiritigenin, an active part and a monomer compound isoliquiritigenin as well as an application of a composition in preparing medicine for treating and preventing triple-negative breast cancer. The composition consists of isoliquiritigenin and one or more active ingredients in gallocatechin, epicatechin and catechin.
WO2006040048A1 Acidic and buffered skin-care compositions comprising nicotinamid and an absorbing agent The invention relates to acidic and buffered skin-care compositions comprising nicotinamid and an absorbing agent, selected from titanium dioxide, titanium dioxide treated with a silicone derivative or fatty acids, zinc oxide treated with a silicone derivative or fatty acids and mixtures thereof. The invention relates also to medicaments comprising said compositions used for treating and/or preventing minor skin irritations, especially diaper dermatitis. The invention relates lastly to the use of said compositions as anti-urease agents.
CN103301466A Hydroprednisone injection composition and preparation method thereof The invention relates to a hydroprednisone injection composition. The per milliliter of composition comprises 4-6mg of hydroprednisone, 0.05-0.15ml of propylene glycol, 0.4-0.6ml of ethanol, 0.1-0.2mg of glycine, 0.2-0.4mg of vitamin B6 and the balance of injection water. The hydroprednisone injection composition provided by the invention has the advantage of extremely high stability.
WO2010151815A2 3,9-diazaspiro[5,5]undecane amides and ureas and methods of use thereof Compounds of formula (I) are useful in treating conditions or disorders ameliorated by α4β2 postive allosteric modulators. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.
US7288650 Protein kinase inhibitors; anticarcinogenic agents; benign prostatic hyperplasia The present invention is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones.
WO2013087643A1 1,3,5 -triazine-2-amine derivatives, preparation thereof and diagnostic and therapeutic use thereof The present invention relates to compounds corresponding to formula (I) in which: - R1 represents a substituted phenyl; - R2 represents: - a substituted phenyl; - a heteroaromatic group, the said group being unsubstituted or substituted one or more times; - R3 represents a group Alk; - R4 represents a hydrogen atom or a (C1-C4)alkyl; - R5 represents a hydrogen atom, a (C3-C6)cycloalkyl or a (C1-C4)alkyl-O-Alk; - or alternatively R4 and R5, together with the nitrogen atom to which they are attached, constitute a heterocyclic radical chosen from: azetidin-1-yl, pyrrolidin-1-yl, piperid-1-yl, morpholin-4-yl; - R6 represents a group -COOAlk, a group -CONH 2 or a group -NHSO 2 Alk; - Alk represents a (C1-C4)alkyl, which is unsubstituted or substituted one or more times with a halogen atom; in the form of the base or of an acid-addition salt. Preparation process and diagnostic and therapeutic use.
US20120142645 Neuroactive steroid compositions and methods of use for lowering cholesterol Methods for ameliorating a symptom associated with hypercholesterolemia, hyperlipidemia, or both in a subject. In some embodiments, the methods include administering to a subject in need thereof an effective amount of a composition comprising pregnenolone (PG), allopregnanolone (ALLO), dehydroepiandrosterone (DHEA), progesterone (PROG), precursors thereof, metabolites thereof, pharmaceutically acceptable salts thereof, derivatives thereof, or combinations thereof. Also provided are methods for ameliorating at least one symptom resulting from undesirable cholesterol biosynthesis in a subject and methods for lowering cholesterol, low density lipoprotein, or both in the serum of a subject.
CN101347568A Formulation of yam pills and quality control method The invention relates to a new preparation of a yam pill and a method for controlling the quality of the preparation. The aim of the invention is to provide a preparation method that: 45g of yam, 21g of eucommia bark (carbonizing by stir-frying), 30g of achyranthes, 105g of liquorice, 9g of aucklandia root, 12g of frankincense (vinegar prepared), 12g of myrrh (vinegar prepared), 9g of homalomena rhizome, 30g of pyritum (vinegar calcined and quenched), 9g of notopterygium root, 9g of anisetree bark, 9g of safflower, 9g of ledebouriella seseloides, 21g of radix dipsaci, 12g of radix bupleuri, 30g of rhizoma cibotii (sand scalded), 60g of Chinese ephedra, 120g of nux vomica powder and pharmaceutically acceptable accessories undergoes the necessary procedure of pulverization, uniform mixing, pellet fabrication, pill fabrication, encapsulation, tablet pressing, etc., and then prepared into pharmaceutically acceptable preparation, such as common tablets, capsules, soft capsules, watered pills, watered-honeyed pills, small honeyed pills, etc. In addition, the aim of the invention is to provide the method for controlling the quality of the preparation, and the new therapeutic applications in the aspects of cervical spondylosis, prolapse of lumbar intervertebral disc, rheumatism, rheumatoid diseases, synovitis, femoral head necrosis, acute myelitis, progressive myatrophy, myasthenia gravis and periodic paralysis.
CN102391192A Preparation method and application of shikimic acid ligustrazine The invention relates to an ion pair compound and a complex of ligustrazine, in particular to a shikimic acid ligustrazine salt and a parathion method and application thereof. The invention provides the ion pair compound with the structural formula (I), the value range of a is 0.1 to 10, and preferably, a is 1 or 2. The shikimic acid ligustrazine salt compound has the pharmacological effect of ligustrazine, and also has the pharmacological effect of shikimic acid; and the compound has good synergistic pharmacological effect on treatment of ischemic cardiovascular and cerebrovascular diseases due to two different pharmacological effects.
US20090162299 Caffeine salt complexes and methods for using the same in the prevention or treatment of cancer The present invention relates to pharmaceutical compositions containing a caffeine salt complex and a pharmaceutically acceptable carrier for use in methods for preventing or treating cancer or solar dermatitis. Methods for inducing apoptosis or inhibiting proliferation in a cancer cell or cell which as UVB-induced DNA damage using a caffeine salt complex or methylated xanthine are also provided.
US20070015755 Novel compounds and compositions as protease inhibitors The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
CN101743240A ((phenyl)imidazolyl)methylheteroaryl compounds Disclosed herein is a compound of the formula wherein A and B are described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
US20120196905 Synthetic compounds and methods to decrease nicotine self-administration Methods and small molecule compounds for smoking and CNS disease harm reduction are provided. One example of a class of compounds that may be used is represented by the compound having the structure IA or IB in the form of free base or a pharmaceutically acceptable salt, hydrate or solvate thereof:
CN102516239A Aromatic thiazole compounds, analogues thereof, uses thereof and preparation methods thereof The invention discloses aromatic thiazole micro-molecular organic compounds with the structural formula represented by formula (I), or hydrates thereof or pharmaceutically acceptable salts thereof. The compounds of the invention or compositions containing the compounds can be used for sun protection, anti-ultraviolet and skin damage protection as a cosmetic additive and for inhibition of the cell apoptosis caused by excess ultraviolet irradiation and the expression of cyclooxygenase COX2. The invention also discloses preparation methods of the aromatic thiazole micro-molecular organic compounds and derivatives thereof.
WO2004015096A8 Leech extracts for stents The invention relates to a stable destabilase complex in the form of a monomer, which is capable of aggregating into a polymer destabilase complex forming a liposome and which can be obtained from medicinal leeches using the following method comprising: affinity chromatography with 6-keto-prostaglandin antibodies which are immobilised on a suitable column; and high ionic strength elution of the destabilase complex, said complex having an antithrombin activity of at least 700 ATU/mg, a plasma recalcification time of at least 800 APC/mg, a fibrinolytic activity of at least 40mm2/mg and an immunomodulating activity.
CN101260108A Mercaptopyrrolidone carbon penems derivatives The invention belongs the medical and pharmaceutical technical field, in particular to novel derivatives of thiol pyrrolidone carbapenem shown in formula (I), as well as pharmaceutically acceptable salts, easily hydrolyzed esters and isomers thereof, and hydrates of the derivatives, and hydrates of the esters or the salts of the derivatives, wherein R<1>, R<2>, R<3> and n are defined in the instruction. The invention also relates to a preparation method for the compounds, combinations containing the compounds, and an application of the compounds to medicines used to treat and/or prevent the contagious diseases.
CN102070656A Substituted imidazole ring-containing cephalosporin derivatives The invention belongs to the technical field of medicines, and particularly relates to a substituted imidazole ring-containing cephalosporin derivatives as shown in the general formula 1 and pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, X and n are defined in the specification. The invention also relates to preparation methods of the compounds, a drug combination containing the compounds and application of the compounds in preparing a drug for treating and/or preventing infectious diseases.
CN102885777A Efficient florfenicol powder composition and preparation method thereof The invention discloses an efficient florfenicol powder composition and a preparation method thereof. The powder composition comprises the following components in percentage by weight: 1-50% of florfenicol, 46-98.9% of a florfenicol-absorbed carrier and 0.05-4% of a florfenicol absorption promoter. The method comprises the following steps of: preparing the raw materials according to the above components; preparing a florfenicol organic solvent solution; dissolving the florfenicol absorption promoter and the florfenicol-absorbed carrier into water to obtain a mixed water solution; and adding the florfenicol organic solvent solution into the mixed water solution, and rapidly spray-drying. The preparation method disclosed by the invention is simple and low in cost. The product disclosed by the invention has the advantages of extrinsic quick release, esoteric quick absorption, high plasma peak concentration, thorough drug absorption and less antibiotic residue. The product disclosed by the invention can be applied to the treatment of infection on all parts of domestic animals caused by bacteria.
CN103012369A Lansoprazole N crystal form and preparation method and application thereof The invention discloses a lansoprazole N crystal form and a preparation method and application thereof. The X-ray powder diffraction of the lansoprazole N crystal form has characteristic peaks when the diffraction angle 2(theta) is 5.438, 7.062, 8.230, 9.216, 11.022, 11.789, 12.610, 13.541, 20.603, 21.862 and 26.242. The preparation method comprises the following steps of: dissolving lansoprazole in ethyl acetate or a mixed solvent of n-butyl alcohol and water; cooling to separate out crystals; and filtering and drying to obtain the lansoprazole N crystal form. The new lansoprazole crystal form disclosed by the invention is easy to prepare; the preparation method requires little solvent and is simple to operate, and the production cost is low; the reaction conditions are mild, and the control is easy; and the reproducibility is good, and a target product crystal form can be stably obtained. Through the method disclosed by the invention, the prepared lansoprazole crystal form has high purity and low impurity content, maintains all pharmacologic characteristics of lansoprazole, and can be used for treating gastric ulcer, duodenal ulcer and reflux esophagitis and eradicating helicobacter pylori.
WO2011131636A1 Combined treatment of cancer with benzo[e]pyridoindoles and dna-damaging agents The present invention relates to a pharmaceutical composition, kit or combined preparation comprising benzo[e]pyrido indoles and DNA-damaging agents, said composition, kit or combined preparation being useful for treating cancer. It also relates to the combinated treatment of cancer with benzo[e]pyrido indoles and radiotherapy.
CN102596201A Dosage regimens for hcv combination therapy comprising bi201335, interferon alpha and ribavirin The present invention relates to therapeutic combinations comprising (a) Compound (1), or a pharmaceutically acceptable salt thereof, as herein described, (b) an interferon alfa and (c) ribavirin and particular regimens for administering this combination. Compound (1) is a selective and potent inhibitor of the HCV NS3 serine protease. The present invention also relates to methods of using such therapeutic combinations for treating HCV infection or alleviating one or more symptoms thereof in a patient.
US20060040988 antiinflammatory, antipyretic and analgesic agents; side effects redution; N-(cyclohexylmethyl)-6-[4-(methylsulfonyl)phenyl]-4-(trifluoromethyl)-2-pyridinamine; osteoarthritis; rheumatoid arthritis Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.
CN1887265A Slow released anticancer prepn The slow released anticancer injection consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is the composition of fotemustine, nimostine, carmustine, bendamustine, etc. The slow releasing supplementary material is polylactic acid and its copolymer, polyethylene glycol-polylactic acid copolymer, EVAc, etc. The .suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent. The present invention has lowered systemic reaction and raised local concentration for 30-50 days, and may be used alone effectively and in enhancing the curative effect of chemotherapy, radiotherapy and other non-operative treatment.
WO2013117348A1 Agonists and antagonists of toll-like receptor (tlr) 13 The present invention relates to the field of immunology. The present invention provides agonists and antagonists of Toll-like receptor (TLR) 13. In particular, the present invention provides TLR13 activating and inhibiting nucleic acids, and provides such nucleic acids for use as pharmaceutical agents. The present invention further provides in vitro methods using such nucleic acids.
WO2008101354A1 Gpr65 as a therapeutic target in allergic airway inflammation The disclosure identifies GPR65 as a protein target involved in the pathophysiology of allergic inflammation and describes a method for treating allergic inflammation by attenuating GPR65 expression or activity. GPR65 expression is shown to be significantly upregulated in a mouse model of allergic airway inflammation, and GPR65-deficient mice are demonstrated to display attenuated eosinophilia and IL-13 levels in response to an allergic challenge. The application further discloses that delivery of GPR65-specific antisense oligonucleotides, that are capable of reducing GPR65 expression in the lung, attenuate airway inflammation in response to allergic challenge.
US20110281946 Polymeric -based composition The present invention concerns polymeric-based compositions that are useful in the delivery and sustained release of hydrophobic therapeutic and/or cosmetic agents substantially at the point of injury, infection or, in the case of purely cosmetic applications, the point of treatment. Also provided are methods of preparing such compositions and methods of treatments involving the use of such compositions.
WO2012164356A1 A method of managing hypercortisolemia, headache disorders, neuropathic pain and related disorders The present disclosure relates to treatment and management of Cushing's syndrome, Headache disorders and Neuropathic using a composition comprising asiaticoside and madecasosside optionally along with at least one excipient. The treatment can be extended to Myalgia and other related disease conditions.
CN103405553A Solid-gel ultra-refreshing fragrant refreshing agent and preparation method thereof The invention discloses a solid-gel ultra-refreshing fragrant refreshing agent and a preparation method thereof. The solid-gel ultra-refreshing fragrant refreshing agent is prepared from, by mass, 0.75-1.50% of an ultra-refreshing fragrance, 0.50-1.50% of solid gel, 8.00-10.00% of a high-efficiency solubilizer, 0.40-0.60% of a preservative, and balance of distilled water. The preparation method comprises ultra-refreshing fragrance preparation, ultra-refreshing fragrance solubilizing, preparation of solid gel with pH of 6-7, mixing of the solubilized ultra-refreshing fragrance and the solid gel with pH of 6-7, and the like, such that the solid-gel ultra-refreshing fragrant refreshing agent is finally obtained. The solid-gel ultra-refreshing fragrant refreshing agent is a pure natural, non-toxic, no-harm, and safe product with effects of fatigue dispelling, depression resisting, and emotion calming. The agent can be smeared on human skin, and can provide a refreshing effect. With the agent, refreshing, cooling, and pleasant fragrance can be continuously released.
CN102432647A Aminoglycoside compound and extracting separation method thereof The invention relates to an aminoglycoside compound and an extracting separation method thereof. The compound is separated from etimicin sulfate and has a following structural formula. The invention also relates to a separating method for the aminoglycoside compound.
CN101874817A Brucea javanica oil enteric-coated microcapsule, preparation method and application thereof The invention belongs to the technical field of medicines and foods, relates to an enteric-coated microcapsule of an oily medicine or food, a preparation method and application thereof, in particular to the brucea javanica oil enteric-coated microcapsule, the preparation method and application thereof. The preparation method comprises the following steps: adding lecithin and an antioxidant to brucea javanica oil to absorb the oil to porous starch so as to obtain an oily soft material; adding an adhesive to the oily soft material, stirring at a high speed, granulating and then sieving to obtain a core material; and finally placing the core material in a bottom-spraying fluidized bed, and then spraying enteric-coated coating liquid to obtain the enteric-coated microcapsule. The brucea javanica oil enteric-coated microcapsule can conceal stench of the brucea javanica oil, avoid nausea and gastric stimulation, is easier to accept by patients, and has stability better than that of oral emulsion and more stable and regular drug release compared with single capsule; and the brucea javanica oil enteric-coated microcapsule and a further preparation thereof are applicable to treatment of various cancers such as lung cancer, brain metastasis, liver cancer and the like and adjunctive treatment after radiotherapy and chemotherapy.
CN101157692A Berberinc derivatives, preparation method and medicinal composition and usage thereof The invention relates to a novel berberine derivative by the modification of the structure of the existing berberine (BBR), the berberine derivative is a compound which is represented by the general formula (I), R in the general formula (I) represents sugar or sulfonic acid group, and the experiments prove that the compound is a precursor of the berberine. The invention also relates to a preparation method of the compound, the pharmaceutical composition by taking the compound as the active ingredient, and the application of the compound and the pharmaceutical composition in the preparation of the drugs for the treatment of type 2 diabetes and the regulation of blood glucose and blood lipids.
WO2007049587A1 Enteric-coated preparation Disclosed is an enteric-coated preparation comprising, as an active ingredient, a therapeutic agent for thrombosis or the like which has a potent inhibitory activity on thrombin, particularly [(S)-1-[(S)-2-[(trans-4-aminocyclohexylmethyl) carbamoyl]pyrrolidine-1-carbonyl]-2-isopropylthio-2- methylpropyl]carbamic acid propyl ester or a pharmaceutically acceptable salt thereof. The preparation is hardly susceptible to the influence of diets, can be administered at a dose frequency of once a day, exerts an effectiveness as a therapeutic agent for thrombosis or the like when orally administered, and has excellent pharmacokinetic properties.
CN200951142Y Copper 300 intrauterine contraception A copper 300 intrauterine device includes a core rod (1) and a body frame (2) which is connected with one end of the core rod (1), a copper wire layer (3) is winded on the core rod (1) and the lower end of the core rod (1) is provided with a copper cover (4). A drug-containing rod (5) may also be arranged on the core rod (1). The total outer surface area of the copper wire layer (3) and the copper cover (4) is 300 square millimeters. The intrauterine device has more reliable contraceptive effect, better flexibility and can reduce the stimulation to the endometrium and reduce the side effects of ringing; in addition, the utility model is more beautiful and smart.
CN1864695A Clathrate consists of astragaloside and cyclodextrin, its preparation method and application The present invention relates to one kind of clathrate of astragalosie A and cyclodextrin derivative. The clathrate of astragalosie A and cyclodextrin derivative consists of astragalosie A and cyclodextrin derivative in the weight ratio of 1 to 1-150. It is prepared through the reaction of astragalosie A and cyclodextrin derivative, filtering the reacted solution with microporous filtering film to separate out the clathrate from the mixture; or through a high energy grinding process. The clathrate of astragalosie A and cyclodextrin derivative has obviously improved water solubility of astragalosie A and may be used in preparing various kinds of liquid preparation for meeting the clinical requirement.
US20090275515 2-hydroxy-2-phenylthiophenylpropionamides as androgen receptor modulators Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HFV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
DE10331350A1 Inhalation powder useful for treating respiratory diseases comprises a 9,9-dimethyl-7-(2,2-diphenylpropionyloxy)-3-oxa-9-azatricyclononane salt and a finely divided excipient Inhalation powder comprises a 9,9-dimethyl-7-(2,2-diphenylpropionyloxy)-3-oxa-9-azatricyclo(3.3.1.0 2.6)nonane salt (I) in admixture with an excipient having an average particle size of 10-50 micro m. - Inhalation powder comprises a 9,9-dimethyl-7-(2,2-diphenylpropionyloxy)-3-oxa-9-azatricyclo(3.3.1.0 2.6)nonane salt (I) of formula 1 in admixture with an excipient having an average particle size of 10-50 micro m. - X = an anion. - Independent claims are also included for: - (1) capsule containing an inhalation powder as above; - (2) kit comprising a capsule as above and an inhaler. - ACTIVITY - Antiasthmatic; Respiratory-Gen. - MECHANISM OF ACTION - Anticholinergic.
US20110263535 Tyrosine-based prodrugs of antiviral agents A tyrosine-based (phosphonylmethoxyalkyl)purine or -pyrimidine conjugate is provided. In some embodiments, the conjugate includes tyrosine based amino acid or dipeptide moieties of (S)-9-(3-hydroxy-2-phosphonyl-methoxypropyl)adenine or its cytosine analogue. A method of synthesizing such conjugates based on Boc-protected amino acid or dipeptides is also provided. In addition, a method of isomerizing an (S,S)-diastereoisomer to an (S,R)-diastereoisomer of an amino acid-based or dipeptide-based conjugate by a process including transesterification is provided. A method of inhibiting viral infection and a method of treating viral infection based on (phosphonylmethoxyalkyl)purine or -pyrimidine conjugates is also provided.
CN103664840A Application of Inula wissmanniana lactone A and derivatives in preparing antiinflammatory drugs The invention relates to the technical field of medicine. The invention provides an Inula wissmanniana lactone A and derivatives thereof, of which the chemical structure is disclosed as general formula I. The invention also provides application of the Inula wissmanniana lactone A and derivatives in preparing antiinflammatory drugs. The compounds can severely inhibit the macrophage RAW264.7 from generating NO, can obviously inhibit the ear swelling and foot swelling of experimental animals in dimethylbenzene induced ear swelling mouse and Freund complete adjuvant arthritis rat models, has favorable antiinflammatory activity, and can be used for preparing antiinflammatory drugs.
EP1983975A2 Method of treatment for muscular dystrophy The invention relates to a method of treatment for muscular dystrophies, including Duchenne, Becker, limb-girdle, facioscapulohumeral, congenital muscular dystrophies and the like using a combination of nitric oxide-releasing and anti-inflammatory compounds.
WO2009061228A1 Chemical preparation for gradually removing benign lesions Chemical preparation for gradual removal of benign lesions and procedure of its application of the facial, head and body skin is the preparation based on formulation of a sintergetic mixture of the following chemical composition: 19.40-40.74% acetic acid, 3.15-7.43% nitric acid, 0.93-4.00% silver nitrate, 0.93-1.96% salicylic acid, 0-2,8% Mg2+, 0-2,3% Cu2+, 0-2,7% Fe3+, 0.5-6.2% dimethylgloxime, 0.3-17.2% trichloroacetic acid and 19.63-56.78% distilled water. The mixture obtained in this way is precisely applied using specially shaped glass microcapillary or similar specially designed device at the volume ranging between 1-10-6cm3 and 3-10-2cm3 on the benign lesion on the facial, head or body skin. The crust that will be formed within the following 72 hours in the treated site, which should not come into contact with water, will spontaneously fall-off within 10 to 40 days. After complete removal of the lesion the new skin will develop on the treated site and its color and appearance will become the same as color and appearance of the surrounding tissue with unnoticeable residual traces. Two months after treatment and falling-off of the last crust the treated site may be cared as all other facial, head and body skin areas using skin-care preparations.
EP1204669B1 Tricyclic monosaccharide derivatives useful in treating acute ischemia-induced neurodegeneration Anticonvulsant compounds of general formula (I) where X, R1, R2, R3, R4, R5, and R6 are as herein defined; are useful in treating acute ischemia-induced neurodegeneration, such as occurs during and after stroke, head trauma, spinal injury, non-fatal cardiac arrest, or major surgical procedures. Furthermore, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use are disclosed.
EP0566709B3 Composition comprising a tramadol compound and acetaminophen, and its use This invention relates to a composition comprising a tramadol material and acetaminophen, and its use. As used herein tramadol refers to various forms of tramadol. The compositions are pharmacologically useful in treating pain and tussive conditions. The compositions are also subject to less opioid side-effects such as abuse liability, tolerance, constipation and respiratory depression. Furthermore, where the components of the compositions are within certain ratios the pharmacological effects of the compositions are superadditive (Synergistic).
CN102240279A Piglet soothing agent and preparation method and application thereof The invention relates to a piglet soothing agent belonging to the field of animal welfare. The piglet soothing agent comprises the following components in percentage by weight: 1.0-3.0% of n-capric acid, 3.0-7.0% of dodecanoic acid, 4.0-8.0% of myristic acid, 8.0-12.0% of hexadecanoic acid, 35.0-40.0% of cis-9,cis-12-octadecadienoic acid, 25.0-30.0% of octadecenoic-cis-9-acid and 15-24% of absolute ethanol. The invention also discloses a preparation method and application of the piglet soothing agent. In addition, the invention also discloses a piglet soothing agent release box which comprises a box body and a box cover, wherein gas scattering pores are formed on the box cover. The piglet soothing agent provided by the invention can significantly reduce the saliva cortisol levels of weaned piglets, slow down the weaning stress of the piglets and obviously reduce the aggressive behavior incidence of the weaned piglets; and in addition, the piglet soothing agent has the advantages of convenient sources of raw materials, no toxicity and harm, no residue and safe and is convenient to use.
EP1839677B1 Adjuvant of fluorocarbon emulsions for hifu therapy and the use thereof An adjuvant of fluorocarbon emulsions for HIFU therapy, which can increase energy deposition in target regions during the therapy, comprises a discontinuous phase consisting of a core encapsuled by a film-forming material and a continuous phase consisting of aqueous medium, wherein the discontinuous phase is well distributed in the continuous one; the particle size of the discontinuous phase is 0.1-2µm; the amount of the film-forming material in the adjuvant is 0.1-100g/L; the core material used is a liquid which performs the liquid-gas phase transition at 38-100°C and is incorporated into the adjuvant in the amount of 5-200ml/L. The adjuvant of fluorocarbon emulsions for HIFU therapy is capable of upgrading the acoustic environment of target regions remarkably, increasing energy deposition in target tissues during HIFU therapy, and consequently significantly improving the damaging effect against tumor cells during clinical HIFU. And the usage of such adjuvant in HIFU therapy.
US20080261862 Integrin mediates proliferative signal provided by CD23 to pre-B cells; immobilized rodent cells; drug screening; anticancer agents; antiinflammatory agents It is disclosed that the αvβ5 integrin mediates the proliferative signal provided by CD23 to pre-B cells. The region of CD23 which interacts with αvβ5 has been defined, and found to interact with a site on the integrin distinct from that which binds RGD. The invention provides methods for disrupting the interaction between CD23 and αvβ5 and methods of screening for chemical entities capable of disrupting this interaction.
WO2010032771A1 Amino acid derivative Disclosed is a novel amino acid derivative having excellent analgesic activity. The amino acid derivative is a novel compound which exhibits excellent analgesic activity not only with respect to nociceptive pain model animals, but also with respect to neuropathic pain model animals, and is extremely useful as a medical agent for the treatment of various painful conditions that exhibit acute or chronic pain or neuropathic pain.
EP1677774B1 Citicoline-based composition in combination with vitamins for the prevention and treatment of eye pathologies A pharmaceutical and/or nutritional composition based on a choline donor compound, preferably citicoline, in combination with vitamin A and vitamin B6. The composition is effective, also upon oral administration, in preserving and restoring the proper structural and functional characteristics of eye tissues in degenerative ophthalmic pathologies, such as glaucoma and am blyopia, in particular. The composition may also include vitamin E and vitamin C.
WO2014008295A1 Manufacture of 2- (5- bromo-4 (-cyclopropylnaphthalen-1-yl) -4h-1,2,4-triazol-3-ylthio) acetic acid Described herein are certain processes for the synthesis of compounds of Formula (I):
CA2203652C A method of down-regulating gene expression Disclosed is a method of down-regulating the expression of a gene in an animal, wherein a pharmalogical formulation comprising an oligonucleotide complementary to the gene is orally administered to an animal. The oligonucleotide administered has non-phosphodiester internucleotide linkages and includes at least one 2'-substituted ribonucleotide, the oligonucleotide inhibiting the expression of a product of the gene, thereby down-regulating the expression of the gene.
US7338672 Administering Leucojum aestivum plant extract containing galanthamine for improving Estrogen-deficiency related cognitive dysfunction Estrogen-deficiency related cognitive dysfunction may be improved by administering a composition comprising an herbal composition to a woman. In a preferred embodiment the herbal composition comprises whole plant extract of Leucojum aestivum.
US20110263573 Heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes The present invention relates to heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
CN101796017A (carboxylalkylene-phenyl)-phenyl-oxalamides, method for the production thereof, and use of same as a medicament The invention relates to bis-phenyl-oxalamides and the physiologically compatible salts thereof. The invention also relates to compounds of formula (I), wherein Rl, R2, R3, R4, R5, R6, R7, R8, m and X have the cited designations, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for the treatment of diabetes.
US20110268683 Structured suspending systems A pourable ringing gel surfactant composition comprising a mixture of at least one anionic surfactant having a C8-C18 carbon chain and at least one zwitterionic or amphoteric surfactant having a C8-C18 carbon chain, wherein the ringing gel is capable of suspending solid or liquid particles without sedimentation.
WO2014075124A1 Methods and compositions for the treatment and/or prevention of bowel disorders The present invention relates to methods for the treatment and/or prevention of bowel disorders. The methods and compositions disclosed herein are useful in treatment and prevention of inflammatory bowel disease.
US20100311728 Manipulation of brain CDP-diacylglycerol and uses thereof Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.
CN103705526A Liquid used for treating rhinitis, diminishing inflammation, and relieving pain The invention discloses an externally applied liquid used for treating rhinitis, and belongs to the field of paranasal sinus and frontal sinus inflammation treatment. The liquid is prepared by mixing ephedrine and furacilin nasal drop, chloramphenicol eye drop, and dexamethasone sodium phosphate eye drop according to a ratio of 10:8:5. The liquid used for treating rhinitis, diminishing inflammation, and relieving pain, is simple in application method, is convenient for using, is safe and effective, is low in side effect, is capable of relieving pain of rhinitis patients, and is verified via years of clinical use; and curative effect is achieved quickly.
CN102379896A Medicine composite for dehydrating, shrinking and eliminating lesion tissues The invention discloses a medicine composite for dehydrating, shrinking and eliminating lesion tissues, wherein inorganic polymer ferric salt and/or inorganic polymer ferric salt composite are/is used as the active ingredients of the medicine composite; and the inorganic polymer ferric salt can be polyferric sulfate (PFS), and the inorganic polymer ferric salt composite can be selected from polymerization silicic acid composite ferric salt, polymerization phosphoric acid ferric salt and/or other similar objects. The medicine composite is utilized to dehydrate, shrink and eliminate the lesion tissues for being further absorbed or fell off, accordingly, the lesion tissues can be restrained, and an unexpected effect is obtained. The medicine composite has low price, obvious curative effects and convenience in use, and can effectively cure piles, hemangioma, varix, cyst, abscess, tumour, scald and fire burn, trauma bleeding, microorganism and chemical toxicant local damage and the like.
WO2014147611A1 Quinolines derivatives as novel anticancer agents The invention provides quinoline derivatives, their manufacture, pharmaceutical compositions containing them, and their use as medicaments. The active compounds of the present invention are useful for the treatment of proliferative neoplastic and nonneoplastic diseases.
US20080194638 Bioavailable formulations of heterocyclic compounds The present invention relates to bioavailable pharmaceutical formulations of heterocyclic compounds, such as such as N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide (oglemilast) and pharmaceutically acceptable salts thereof, to processes for their preparation and to methods of treatment using the same. The present invention also relates to substantially pure amorphous forms of heterocyclic compounds, such as oglemilast. The invention is particularly directed to bioavailable pharmaceutical oral dosage forms containing amorphous oglemilast.
US20120122950 Libraries of 1-(sulfonyl)-n-phenylpyrrolidine-2-carboxamides for drug discovery New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to 1-(sulfonyl)-N-phenyl-pyrrolidine 2-carboxamides which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.
WO2014151853A1 Methods of treating bladder cancer The present invention provides methods and compositions for treating bladder cancer, including metastatic bladder cancer and non-muscle-invasive bladder cancer, by administering a composition comprising nanoparticles that comprise mTOR inhibitor and optionally an albumin.
WO2009065226A1 Modulation of tdag51 to inhibit scar formation in skin wound healing and internal organ fibrosis Methods and compositions for the modulation of wound healing, scar formation and organ fibrosis are provided. The methods and compositions involve modulation of the T cell death associated gene (TDAG51) and/or the related protein. The modulation of TDAG51 expression and/or activity may be effected by genetic or pharmacological means.
EP0964864B1 Pyrido 2,3-d pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2-(amino and thio)pyrido[2,3-d]pyrimidines and 4-aminopyrimidines that are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention provides compounds of Formula (I) and Formula (II), where W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R?8 and R9¿ include hydrogen and alkyl, and Z is carboxy. This invention also provides pharmaceutical formulations comprising a compound of Formula (I or II) together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.
WO2014099676A1 Chloro-pyrazine carboxamide derivatives useful for the treatment of diseases favoured by insufficient mucosal hydration This invention provides compounds of the formula (I) and their pharmaceutically acceptable salts, useful as sodium channel blockers, compositions containing the same, therapeutic methods and uses for the same and processes for preparing the same.
CN101164584A Method for making lung-moistening and throat-clearing lozenge The present invention relates to a preparation method of lung-moistening pharynx-clearing lozenge. Said preparation method uses menthol, borneol, licorice, solidago, watermelon frost, scrophularia root and platycodon root as raw material and adopts the following steps: mixing above-mentioned raw materials according to a certain mixing ratio, adding water to make extraction, filtering, concentrating filtrate, drying, pulverizing to obtain powdered material for stand-by; melting white sugar and maltose, mixing the molten white sugar and maltose with the above-mentioned powdered material and making them into the invented lozenge.
WO2009094168A1 Cxcr3 antagonists Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis, transplant rejection and type I diabetes.
US7019013 Sulfamidothienopyrimidines The invention relates to compounds of the formula (I) in which R1, E2 and X are as defined above.
CN102614310A Dehumidifying lotion for treating keratosic dermatosis and preparation method thereof The invention discloses a dehumidifying lotion for treating five kinds of keratosic dermatosis. The dehumidifying lotion is prepared from the following raw materials in parts by weight: 30 parts of cowherb seed, 30 parts of garden balsam stem, 30 parts of sophorae flavescentis, 30 parts of cortex lycii radicis, 30 parts of cortex dictamni, 10 to 20 parts of safflower and 10 to 20 parts of alum. The raw materials are mixed and conventionally decocted in water, 15 to 20 minutes after decoction, the decoction is naturally cooled until the decoction does not scald hands, and a wounded part is soaked in the decoction for 20 to 30 minutes at each time and is soaked for 1 to 2 times each day, wherein a treatment course is two weeks. The dehumidifying lotion has the effects of clearing heat and removing toxicity, dispelling wind and arresting itching, softening ceratine, removing rot and generating muscles, and the like, is obvious in treatment effect and quick in effect and does not have adverse reaction.
US20090137565 Method for treatment of movement disorders The invention is directed to methods of treating movement disorders by administering an effective amount of the compound of formula (I) to patients in need thereof. More particularly, the invention is directed to a method for treating myoclonus including administering to a patient a compound of formula (I), wherein the myoclonus is not alcohol responsive essential myoclonus with dystonia. In some embodiments, the myoclonus is posthypoxic myoclonus. The invention is also directed to a method for treating dystonia, essential tremor cerebellar tremor, a tic, or chorea, including administering to a patient a compound of formula (I).
CN103006895A Preparation of lithontriptic capsule The invention provides an oral lithontriptic capsule, which consists of agaric, chicken gizzard-membrane, lygodium japonicum, talcum powder, longhairy antenoron herb and belladonna. The preparation process of the capsule comprises the following steps of: deslagging the six drugs; extracting effective ingredients, and mixing in a certain proportion, which means crushing and uniformly mixing; and filling into capsules with 300mg in each capsule. The lithontriptic capsule can be used for treating various types of stones, and has the advantages of remarkable curative effect, simplicity in preparation, convenience in use, low price and the like.
US20080089911 Borrelia burgdorferi outer surface protein ( OSP)C antigen and a second antigenic lipoprotein such as genetic engineered OSPA, or streptococcus pneumoniae cell surface protein ( PSPA) or both in same physio-chemical Immununological compositions and methods for making and using them. The compositions contain at least one antigen and at least one lipoprotein and optionally an adjuvant. The lipoprotein can itself be antigenic or immunogenic. The antigen can be influenza HA and the lipoprotein a recombinantly expressed product having an OspA leader for lipidation and PspA for the protein portion. The antigen can be OspC and the lipoprotein OspA. The components of the composition are co-administered. A potentiated immunological response is obtained by the compositions and methods.
EP1187598B1 Micropigment mixture The invention relates to the use of mixtures of micronized organic UV filters for the protection of the human and animal skin and hair from the detrimental effects of UV radiation. The invention also relates to the use of said mixtures in cosmetic and pharmaceutical formulations. The micronized mixtures used according to the invention cover a broad UV range and therefore have excellent sun protection properties.
US20050143423 Antiulcer; antisecretory; solubility, bioavailability; slow hydrolysis; full inhibition of acid secretion in oral therapy by prolonged presence in body; 1-(carboxythiophenesulfonyl)- 2-(substituted pyridylmethylsulfinyl) benzimidazoles; also with LANSOPRAZOLE, OMEPRAZOLE, PANTOPRAZOLE, or RABEPRAZOLE Prodrugs of proton pump inhibitors of Formulas 1 through 4, where the symbols are as defined in the specification, and the R group includes at least one acidic group or its pharmaceutically acceptable salt, have improved aqueous solubility and bioavailability.
CN101632641B Lentinan lyophilized power injection and preparation method thereof The invention relates to a lentinan lyophilized power injection and a preparation method thereof, belonging to the technical field of biological response modifier antitumor drugs. The lentinan lyophilized power injection is characterized in that the injection comprises 0.95-1.10 parts of lentinan and 1-33.5 parts of excipient by weight, wherein the weight mean molecular weight of lentinan is 400-800 thousands, the content of the components with more than 20 thousands is not less than 98wt% and the content of the components with more than 2000 thousands is less than 2wt%, the invention has theadvantage that salt-free technology is used in the preparation method of the lyophilized preparation and water for injection is used for direct dissolution in the preparation of the injection. The salt-free preparation can reduce the adverse reaction of patients and improve the safety of medication. The invention ensures the curative effect of lentinan, reduces the poison and side effect, increases the safety and reduces the production cost and the preparation method is simple and is applicable to scale industrialized production.
CN102846558A Lornoxicam freeze-drying preparation and preparation method thereof The invention discloses a lornoxicam free-drying preparation and a preparation method thereof. The lornoxicam free-drying preparation comprises the following raw materials by weight part: 1 part of lornoxicam, 2.3-3.5 parts of poloxamer 188, 10-15 parts of mannitol, 0.01-0.025 part of EDTA (Ethylene Diamine Tetraacetic Acid)-CaNa, proper amount of 1mol/L NaOH, and 230 parts of water for injection. The lornoxicam freeze-drying preparation disclosed by the invention takes the poloxamer 188 as a cosolvent, takes sodium hydroxide as a PH adjusting agent, and has the characteristics of improving the dissolving speed of lornoxicam, ensuring the stability and solubility, and being simple and convenient in sample preparing process, and suitable for large-scale production.
CN103417639A Quick-acting sore throat powder The invention discloses quick-acting sore throat powder. The quick-acting sore throat powder comprises, by weight, 5-8 grams of amber, 5-8 grams of acacia catechu, 8-12 grams of cinnabar, 6-10 grams of pearl, 6-12 grams of borax, 3-6 grams of realgar, 2-5 grams of borneol, 2-5 grams of bezoar, 5-8 grams of natural indigo, 10-16 grams of radix sophorae tonkinensis and 5-9 grams of lotus leaves. A method for preparing the quick-acting sore throat powder includes respectively grinding the amber, the acacia catechu, the cinnabar, the pearl, the borax, the realgar, the borneol, the bezoar, the natural indigo, the radix sophorae tonkinensis and the lotus leaves to obtain powder; sieving the powder by sieves to obtain fine powder; proportioning and synthesizing the powder in grams; uniformly stirring the fine powder to obtain the powdery medicine for standby spraying. The quick-acting sore throat powder has the advantage that the medicine can be used for quickly treating throat diseases, membranous stomatitis of children, mycotic stomatitis, acute tonsillitis, laryngalgia diseases, acute laryngeal infection, epidemic throat diseases, hoarse throat, throat aphthae, throat tinea, laryngeal mushroom, diphtheria, early tongue symptom of scarlet fever, and the like.
US7348017 such as 2-[Benzyl[(4-methoxyphenyl)sulfonyl]amino]-N-(3-thioxo-3H-1,2,4-dithiazol-5-yl)acetoamide; cosmetics; antiaging agents A dithiazole compound or a salt thereof is disclosed. The compound inhibits matrix metalloprotease (MMPs) activity and can be used in pharmaceutical and cosmetic compositions for the treatment of skin conditions.
EP1663185A1 Prevention and treatment of inflammation-induced and/or immune-mediated bone loss The present invention relates to the use of an 11-ß-HSD-type 1 and/or type 2 inhibitor for the manufacture of a pharmaceutical agent for the prevention and/or treatment of inflammation-induced and/or immune-mediated loss of bone and/or cartilage.
US20110054031 Ophthalmic NSAIDS as Adjuvants The disclosure provides methods and ophthalmic NSAIDs as adjuvants to VEGF inhibitors useful for treating retinal disorders, including but not limited to wet AMD, diabetic retinopathy, diabetic macular edema, central retinal vein occlusion, and branch retinal vein occlusion.
CN102068689A Swine alum powder The invention discloses a formula of a hereditary externally applied medicament for treating otitis media, namely swine alum powder and a preparation method thereof. The swine alum powder is prepared from swine gall (boar gall), calcined alum, sulfanilamide powder, borneol and chymotrypsin according to a certain proportion. The using method comprises the step of using a beverage straw to blow the medicament into a cleaned sick ear once or twice a day. The swine alum powder has remarkable effect of treating the otitis media, is convenient to use and has no toxic or side effect; the effective rate is 100 percent; the cure rate is 96 percent; and the medicament is the swine alum powder worthy of promotion.
US20080193489 Personal Lubricant Compositions That Are Free Of Glycerin and Parabens A stable personal lubricant composition comprising xylitol and excluding glycerin and parabens is provided. In one embodiment, the composition comprises from about 1% to about 15% by weight xylitol; from about 10% to about 35% by weight butylene glycol; from about 5% to about 20% by weight propylene glycol; from about 0.1% to about 1.0% by weight polyquaternium; and from about 50% to about 70% by weight water. Also provided are methods of making and using the personal lubricant compositions comprising xylitol. Packaged kits of the compositions and articles of manufacture including the personal lubricant compositions comprising xylitol also are provided.
WO2007086082A3 A process for manufacturing rosuvastatin potassium and crystalline and amorphous forms thereof A process of manufacturing of Rosuvastatin Potassium of formula (1) is disclosed. The process comprises the steps of (a) treating Rosuvastatin protected compound of formula (II) wherein R1 and R2 are same or different having C1-C4 carbon atom or hydrogen or R1 and R2 can combine together to afford a cyclic structure comprising a junction atom as carbon or metal atom such as Si (silicon); with an inorganic base of the kind such as herein described having potassium as cation in a suitable solvent to form Rosuvastatin potassium; (b) isolating Rosuvastatin potassium.
US20080027119 Methods and compositions employing bicifadine for the treatment of acute pain, chronic pain, and symptoms of neuropathic disorders Methods and compositions are provided for formulating and administering bicifadine and related compounds to treat acute pain, chronic pain, and symptoms associated with neuropathic disorders.
US20120115864 Substituted Fused Pyrimidine Compounds The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
WO2009106534A1 Novel heterocyclic carboxamides as m1 agonists The present invention relates to novel M1 agonistic compounds of formula (I) and their use in the treatment of cognitive impairment associated i.a. with schizophrenia and in the treatment of other diseases mediated by the muscarinic M1 receptor.
EP2058008A1 Anti-obesity agent and use thereof Disclosed is a novel anti-obesity agent. Also disclosed is a therapeutic method using the anti-obesity agent. The anti-obesity agent comprises a GABAB receptor agonist or a pharmacologically acceptable salt thereof as an active ingredient.
CA2816285A1 Naphthyridine derivative Provided, for example, are a compound described below and the like, which have amyloid ß production inhibitory activity, especially BACE1 inhibitory effect and serve as therapeutic agents for diseases induced by the production, secretion and deposition of amyloid ß protein. A compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the compound or the salt. (In the formula, ring Z represents a substituted or unsubstituted pyridine or a substituted or unsubstituted carbon ring; ring A represents a substituted or unsubstituted carbon ring or a substituted or unsubstituted heterocyclic ring; R1 represents a substituted or unsubstituted alkyl or the like; and R2a, R2b, R4a and R4b each independently represents hydrogen, a substituted or unsubstituted alkyl or the like.)
US7850984 Administering antagonist to sphingomyelinase gene product;side effect reduction of cancer therapy Described are methods for protecting the female reproductive system against natural and artificial insults by administering to women a composition comprising an agent that antagonizes one or more acid sphingomyelinase (ASMase) gene products. Specifically, methods disclosed herein serve to protect women's germline from damage resulting from cancer therapy regimens including chemotherapy or radiotherapy. In one aspect, the method preserves, enhances, or revives ovarian function in women, by administering to women a composition containing sphingosine-1-phosphate, or an analog thereof. Also disclosed are methods to prevent or ameliorate menopausal syndromes and to improve in vitro fertilization techniques.
US20080255240 Obesity; dietetics; hypotensive agents; antidiabetic agents; dyslipidemia; cardiovascular disorders; osteoarthritis; gall bladder disease; endometrosis; anticancer agents; vascular system disorders; apoptosis Novel sulfon amide derivatives are chemical uncouplers useful e.g. for the treatment of obesity.
US6872730 Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula I: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j and k are defined herein.
CN102988557A Preparation method of leuconychia drop The invention discloses a preparation method of a leuconychia drop. The preparation method comprises the following steps of: (1) respectively taking 50-100 parts of golden cypress, 50-100 parts of radix sophorae flavescentis and 50-100 parts of cocklebur fruit, respectively adding 100 parts of water, carrying out water extraction for 2 hours at a temperature of 90-100 DEG C to obtain extracting solutions; (2) evenly mixing 20-40% of glacial acetic acid and 5-15% of iodine; (3) adding 5-10% of a golden cypress extracting solution, 5-10% of a radix sophorae flavescentis extracting solution and 1-8% of a cocklebur fruit extracting solution into an appropriate amount of ethanol, stirring at the normal temperature and evenly mixing; and (4) mixing the mixtures obtained in the steps (2) and (3), adding ethanol and complementing till 100%, and evenly stirring to obtain the finished product. The leuconychia drop prepared by the invention has a powerful fungicide function and has no toxic and side effects on the human body.
WO2013046041A1 Pyridinylpyrazoles for use as kinase modulators for the treatment of cancer Compounds of the substituted pyrazole class of Formula (I) as treatments for cancer are reported. A method of treating cancer in which a compound that inhibits the activity of receptor kinases is described. Said method is effective and can be provided in addition to standard therapies, notably chemotherapy using cytotoxic drugs and other forms of immune therapy including therapeutic vaccines.
US20130018105 Cis, 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one derivatives, substantially enantiomerically pure compositions and methods The present application provides cis 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one derivatives and substantially enantiomerically pure compositions thereof. These derivatives include (+)-(4S,5R)—3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, (−)-(4R,5S)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, and salts and crystals thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, activate GPR120, inhibit inflammation, and treat conditions responsive to PPARγ modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.
CN101319022A Polystyrene-poly-(vinyl benzene-alternate mannose-based maleic acid), preparation method and application thereof The invention relates to polystyrene-poly (styrene-alternated mannose-based maleic acid), a preparation method thereof and an application of the same, which relates to the polystyrene-poly (styrene-alternated-mannose-based maleic acid) and a medicinal application of the polystyrene-poly (styrene-alternated-mannose-based maleic acid) in the aspects of being taken as an external contraceptive drug and being used for inhibiting HIV-1 infection. The compositions by mass percentage of the polystyrene-poly (styrene-alternated mannose-based maleic acid) are: 30 percent of polystyrene and 70 percent of poly (styrene-alternated-mannose-based maleic acid), wherein, the molecular weight is 22,000. The polystyrene-poly (styrene-alternated mannose-based maleic acid) can be used for preparing the external contraceptive drug and can be used for preparing an external anti-AIDS drug.
CA2121364C Vaccines for actinobacillus pleuropneumoniae Novel vaccines for use against Actinobacillus pleuropneumoniae are disclosed. The vaccines contain at least one A.pleuropneumoniae transferrin binding protein and/or one A. pleuropneumoniae cytolysin and/or one A. pleuropneumoniae APP4. Also disclosed are DNA sequences encoding these proteins, vectors including these sequences and host cells transformed with these vectors. The vaccines can be used to treat or prevent porcine respiratory infections.
CA2285573C A method for stimulating red blood cell production The present invention discloses a method for treating anemia by stimulating red blood cells production by administering parenterally Product R, a peptide-nucleic acid preparation.
CN102924458A 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein XI, X2, X3, X4, X5, X6, X7, R<1>, and Q<1> are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
CN102070555A 3-(2-amino-ethyl)-5-(3-cyclohexyl-propylidene)-thiazoline-2,4-diketone and derivatives thereof The invention provides 3-(2-amino-ethyl)-5-(3-cyclohexyl-propylidene)-thiazoline-2,4-diketone and derivatives thereof. The compounds can be used as a dual inhibitor for Raf/MEK/ERK and PI3K/Akt signaling pathways, and can be used for treating cancer.
US20110230430 Saponin extract from saponaria spp. and uses thereof A saponin extract from Saponaria vaccaria and its use for stimulating apoptosis in cancer cells and treating cancer is described. The saponin extract may be isolated from Saponaria vaccaria seed. The saponin extract may comprise one or more than one triterpene saponin. The triterpene saponin may comprise a bisdesmosidic saponin having a molecular weight selected from the group consisting of molecular weight 1448, 1464, 1422, 1526, 1596 and 1688. Bisdesmosidic saponin of molecular weight 1448, 1464, 1422, 1526, 1596 and 1688 isolated from Saponaria vaccaria seed may be used to treat human cancer including prostate cancer, human breast cancer and colon cancer. Also disclosed is a method of isolating the saponin extract.
US20050187264 2-Cyano-N-[4-(methoxymethoxy)phenethyl]-3-(3-pyridyl)-2-propenamide: generic derivatives described in WO 99/05109; asthma; bronchitis; rhinitis; vision defects; antiarthritic agents; antiallergens; sepsis; inflammatory bowel disease; bipolar disordes; schizophrenia; Crohn's disease; degenerative joints This invention relates to a phosphodiesterase IV inhibitor containing as an active ingredient a pyridylacrylamide derivative represented by the following formula (I): (wherein Ar1 represents substituted or unsubstituted pyridyl; Ar2 represents phenyl substituted by alkoxy, etc.; R1 represents hydrogen, alkyl, or aryl; R2 represents hydrogen, alkyl, cyano, or alkoxycarbonyl; R3 represents hydrogen or optionally substituted alkyl; X represents oxygen or sulfur; A and B are the same or different and each independently represents hydrogen, hydroxyl, alkoxy, or alkylthio, or A and B together represent oxo, thioxo, etc., or A may be hydroxyl and B may be 1-alkylimidazol-2-yl; and n is an integer from 1 to 3) or a pharmaceutically acceptable salt thereof.
US7169761 Azulene derivatives and salts thereof The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.
WO2011014681A1 Poly (ADP-Ribose) Polymerase (PARP) INHIBITORS Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.
WO2010080577A3 Oxepine modulators of h1 receptors and/or inhibitors of mast cell degranulation The present invention relates to new oxepine modulators of H1 receptors and/or inhibitors of mast cell degranulation, pharmaceutical compositions thereof, and methods of use thereof.
US20130034549 Combination therapy for treating breast cancer The invention provides compositions and methods for treating breast cancer. Specifically, the invention relates to administering a Transforming Growth Factor beta (TGFβ) antagonist in combination with capecitabine and ixabepilone to treat breast cancer.
US20110166209 Compositions and methods for ameliorating myosin viia defects The invention provides compositions and methods for ameliorating defects in myosin VIIa (MYO7A) expression and/or function, including providing vectors for myosin VIIa expression and formulations comprising them, and methods of using them, for treating human retinitis pigmentosa (or retinal degeneration), and blindness and deafness such as that found in Usher syndrome. The invention provides in vivo gene therapy for ameliorating defects in myosin VIIa (MYO7A) expression and/or function, including compositions and methods for gene transfer of the human myosin VIIa (MYO7A) gene (the MYO7A gene.
US7820679 N-(-3-methoxy-5-methylpyrazin-2-yl)-2-(4-′1,3,4-oxadiazol-2-yl-phenyl)pyridine-3 sulphonamide as an anticancer agent The use of N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide, or a pharmaceutically acceptable salt thereof, in the treatment of cancer and/or pain in a warm blooded animal such as man is described.
CA2813256A1 Aryl-substituted imidazoles The compounds of the invention are antagonists of MDM2 and MDMX, with excellent specificity for MDM2 and MDMX over other proteins, and with selective binding affinity to MDMX over MDM2. The compounds can therefore regulate p53 activity and treat a variety of cancers. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
CN101417988B Biguanide piperazines dipeptidyl peptidase IV inhibitor The invention belongs to the technical field of medicine, and in particular relates to a biguanide piperazines dipeptidyl peptidase IV inhibitor as shown in a general formula (I), and a pharmaceutically acceptable salt or an isomer thereof, wherein Ar, R<1>, R<2> and R<3> are as defined in the introduction. The invention also relates to a method for preparing the compounds, a pharmaceutical composition containing the compounds, as well as application of the compounds in the preparation of medicine for treating and/or preventing diabetes, non-insulin-dependent diabetes, high blood sugar, and insulin resistance.
US20090156511 Agent for Enhancing Antiseptic Power The present invention relates to a preservative efficacy-enhancing agent capable of allowing an antiseptic agent to exhibit a high preservative efficacy even when the antiseptic agent is used at a low concentration; a preservative efficacy-enhancing composition containing the same; and a method for enhancing a preservative efficacy of antiseptic agents. The present invention relates to: (1) a preservative efficacy-enhancing agent for antiseptic agents which includes an amphiphilic galactose derivative (A) as an effective ingredient; (2) a preservative efficacy-enhancing composition including 0.01 to 30% by mass of an amphiphilic galactose derivative (A) and 0.01 to 1.0% by mass of an antiseptic agent (B); and (3) a method for enhancing a preservative efficacy of an antiseptic composition which includes the step of allowing 0.01 to 30% by mass of an amphiphilic galactose derivative (A) to coexist with an antiseptic agent (B) in the composition.
CA2223397C Novel nor-pregnanes for inducing hypothalamic effects The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a 19-nor-pregnane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.
WO2008000777A3 Phenyl- pyrazole derivatives, process for their preparation and their pharmaceutical use The present invention provides compounds of formula (I), a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation and/or allergic conditions.
CN103462915A Flunarizine hydrochloride tablet and preparation method thereof The invention discloses a flunarizine hydrochloride tablet and a preparation method thereof. The preparation is prepared in the following manner: hydroxypropyl cellulose and flunarizine hydrochloride are dissolved in ethanol, a blank pellet is added, a main drug is wrapped by the hydroxypropyl cellulose and is slowly adsorbed on the surface of the pellet in a slow solvent removal process, and then, the drug-carrying pellet and pharmaceutically acceptable additives are uniformly mixed and are directly tabletted. According to the flunarizine hydrochloride tablet and the preparation method disclosed by the invention, direct contact between flunarizine hydrochloride and the external environment is avoided, thereby eliminating the preparation equipment corrosion problem resulting from strong acidity of the drug in the production process of the preparation.
WO2005003115A1 Thiophene amino acid derivatives, process for preparing them and pharmaceutical compositions containing them Compounds of formula (I), in which: R1 and R2, which may be identical or different, independently of each other, each represent a group selected from: hydrogen, halogen, cyano, nitro, halo(C1-C6)alkyl, halo(C1-C6)alkoxy, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, -OR4, -NR4R5, -S(O)nR4, -C(O)R4, -CO2R4, -O-C(O)R4, -C(O)NR4R5, -NR5-C(O)R4, -NR5-SO2R4, -T-CN, -T-OR4, -T-OCF3, -T-NR4R5, -T-S(O)nR4, -T-C(O)R4, -T-CO2 R4, -T-O-C(O)R4, -T-C(O)NR4 R5, -T-NR5-C(O)R4, -T-NR5-SO2R4, -R6 and -T-R6 in which n, T, R4, R5 and R6 are as defined in the description ; m represents an integer between 0 and 4 inclusive ; p represents an integer between 0 and 4 inclusive ; q represents an integer between 0 and 4 inclusive ; R7 represents a group selected from aryl, cycloalkyl and a heterocycle, each of these groups being optionally substituted; R8 represents a group selected from carboxyl, (C1-C6)alkoxycarbonyl, (C1-C7)acyl, hydroxy(C1-C6)alkylcarbonyl, (C1-C6)alkoxy(C1-C6)alkylcarbonyl, tetrazole, amino, aminocarbonyl and amino(C1-C6)alkylcarbonyl; the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and the pharmaceutical compositions which are useful for treating pathologies associated with an inhibition of metalloproteases.
WO2012072791A3 2-(1-phenyl-4,5,6,7-tetrahydro-1h-indazol-4-yl)ethylamine derivatives useful as sigma receptor inhibitors The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to indazole derivatives of formula I and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and/or prophylaxis, in particular for the treatment of psychosis or pain.
WO2011117264A1 N-(imidazopyrimidin-7-yl)-heteroarylamide derivatives and their use as pde10a inhibitors The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R1, R2 and R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDEIOA and used as medicaments.
CN101068597A Fumarate of 4-((4-(4-(2-cyanoethenyl)-2,6-dimethylphenyl)amino)-2-pyrimidinyl)amino)benzonitrile The present invention concerns methods and compositions of use for treatment of Alzheimer's Disease (AD). In certain embodiments, the methods concern preparation of phage-display single chain antibody libraries and screening against amyloid-beta (Abeta) protein or peptide. Anti-Abeta antibodies are selected and sequenced. In certain embodiments, synthetic Abeta binding peptides are designed and prepared, using portions of the anti-Abeta antibody sequences. The antibodies and peptides are of use for treatment of AD or for treatment of individuals at risk of developing AD. Compositions comprising anti-Abeta antibodies or Abeta binding peptides are also disclosed.
CN103564194A Cordyceps polysaccharide composition, as well as preparation method and application of cordyceps polysaccharide composition The invention discloses a cordyceps polysaccharide composition. A preparation method of the cordyceps polysaccharide composition comprises the steps: 1, inoculating a cordyceps militaris strain after activating in a seed culture medium, culturing at a temperature of 20-30 DEG C for 5-7 days to prepare a seed solution; 2, adding a fermentation culture medium in a fermentation tank, sterilizing, cooling to 25-35 DEG C to obtain a mixture, adding the seed solution which accounts for 2-4 percent of the mixture in volume, stirring and fermenting at a temperature of 20-35 DEG C for 3-7 days; 3, pulping, homogenating and centrifuging a mixture I obtained after fermentation in the step 2 to obtain supernate, and obtain the cordyceps polysaccharide composition. The invention further discloses a production method of the cordyceps polysaccharide composition, and an application to the preparation of a feed or medicine for improving the immunity character of pawns. The cordyceps polysaccharide composition is capable of enhancing the disease resistance of the pawns under a high-density culturing condition. The cordyceps polysaccharide composition provided by the invention is remarkable in effect, simple in production process, low in cost, good in safety and economic benefit, and suitable for industrialized application.
EP1846084A1 Device and method for treatment of wounds with nitric oxide Topical exposure of nitric oxide gas to wounds may promote healing of the wound and prepare the wound bed for further treatment and recovery. Nitric oxide gas may be used, to reduce the microbial infection, manage exudate secretion, upregulate expression of endogenous collagenase to locally debride the wound, and regulate the formation of collagen. Additionally, exposure to the high concentration for a first treatment period reduces the microbial burden and inflammation at the wound site and increase collagenase expression to debride necrotic tissue at the wound site. After a first treatment period with high concentration of nitric oxide, a second treatment period at a lower concentration of nitric oxide may be provided to induce collagen expression aiding in the closure of the wound.
CN103301101A Novel 2-(2-fluorine-4biphenyl)-propionic acid pharmaceutical composition The invention provides a novel 2-(2-fluorine-4biphenyl)-propionic acid pharmaceutical composition. Flurbiprofen and basic amino acid arginine or lysine form a pharmaceutical composition solution. The composition can be administrated in an injection or oral administration manner and can also be further administrated in a freeze-drying manner. Compared with a flurbiprofen axetil injection, a flurbiprofen composition not only does not influence the antipyretic, anti-inflammation and analgestic effects of the flurbiprofen, but also has the advantages of simple technology, low cost, high quality, stable long shelf life and convenience in quality control, storage and transportation; moreover, compared with a conventional oral preparation, the flurbiprofen composition has the same low gastrointestinal tract adverse reaction as the flurbiprofen axetil injection.
WO2011137511A1 Compounds, compositions and methods for treatment of central nervous system injuries The invention relates to compositions comprising 6-phenyl-4-pyridin-4-yl-3-(4-pyrimidin-2-ylpiperazin-1-yl) pyridazine, or a pharmaceutically acceptable salt thereof, and use of the compositions to treat central nervous system injuries such as traumatic brain injury or intracerebral hemorrhage, in a subject.
US20110280927 Composition and dressing with nitric oxide A dressing composition for use as a skin dressing comprises an elastomeric-adhesive composition, and a zeolite comprising releasably adsorbed nitric oxide. The zeolite may comprise a transition metal cation such as Co, Fe, Mn, Ni, Cu, Zn, Ag or a mixture thereof as an extra-framework metal cation, preferably Zn. The elastomeric adhesive composition may be a hydrocolloid-adhesive composition comprising, hydrocolloid and elastomer. The dressing composition releases nitric oxide, which may have beneficial effects, when used on wounds or moist skin, with a substantially constant release rate over a long period of time. A dressing including a layer of the dressing composition has a backing layer and may have a release liner removably attached to the skin-contacting surface of the dressing layer.
US7238694 Rifamycin imino derivatives effective against drug-resistant microbes The present invention relates to rifamycin 3-iminomethylenyl (—CH═N—) derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. The claimed rifamycin derivative has a rifamycin moiety covalently linked to a linker through an iminomethylenyl (—CH═N—) group at the C-3 carbon of the rifamycin moiety and the linker is, in turn, covalently linked to a quinolone structure or its pharmacophore within the DNA gyrase and topoisomerase IV inhibitor family. The inventive rifamycins are novel and exhibit activity against both rifampin and ciprofloxacin-resistant microorganisms.
US20100291074 Cyclophilin d-amyloid beta interaction potentiates mitochondrial dysfunction in a transgenic mouse model of alzheimer's disease The present invention is directed to methods for treating or preventing Alzheimer's disease by administering therapeutically effective amounts of an agent that reduces Cyclophilin D expression in a patient, or that reduce Cyclophilin D activity or its ability to form a complex with Amyloid beta. Such agents include antisense nucleotides and small interfering RNAs, antibodies that selectively bind to Cyclophilin D, and cyclosporine A and D.
WO2011133750A1 Indazole compounds useful as ketohexokinase inhibitors The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and / or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.
CN102085196A Nefopam hydrochloride bilayer slow-release tablet and preparation method thereof The invention relates to a nefopam hydrochloride bilayer slow-release tablet and a preparation method thereof. The nefopam hydrochloride bilayer sustained-release tablet is characterized by being prepared by the step of jointly tabletting a quick release layer and a slow release layer into a bilayer tablet, wherein the proportion of nefopam hydrochloride as the main drug contained in the quick release layer and the slow release layer is (1:1)-(1:5). The invention belongs to the technical field of medical preparations and aims at providing the nefopam hydrochloride bilayer slow-release tablet capable of relieving pain rapidly and relieving and easing pain uniformly and persistently and a preparation method thereof. The bilayer slow-release tablet has the advantages of not only decreasing side effects of a common nefopam hydrochloride preparation to the gastrointestinal tract, but also lowering the medicine-taking frequency of patients, reducing adverse effects and improving patient compliance.
US20120093798 Methods for Treatment of Stroke or Cerebrovascular Methods of using an ETB receptor agonist, such as IRL-1620, for the treatment of stroke or cerebrovascular accidents are disclosed. The ETB receptor agonist is used alone or in combination with a second agent useful in the treatment of stroke or other cerebrovascular accident.
EP1735277B1 2-alkylidene-18,19-dinor-vitamin d compounds 2-alkylidene-18,19-dinor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by low bone calcium mobilization activity and high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis, as well as autoimmune diseases such as multiple sclerosis, diabetes mellitus and lupus. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis. These compounds also increase both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.
US20080044353 Combination Therapy for Weight Management Compositions and methods are provided for weight management. The compositions generally comprise a MCHR antagonist, either in combination with a CB1 antagonist or formulated for coadministration with a CB1 antagonist. Certain methods involve coadministering a MCHR antagonist and a CB1 antagonist to a patient.
CN102488680A Ibuprofen diphenhydramine dispersing tablet and preparation method thereof The invention provides an ibuprofen diphenhydramine dispersing tablet, which consists of the following components in percentage by mass: 40 percent of ibuprofen, 5 percent of diphenhydramine hydrochloride or 7.6 percent of diphenhydramine citrate, 30-43 percent of a filler, 5-15 percent of a disintegrant, 2-8 percent of a bonding agent, 0.1-1 percent of a surfactant, 1.5-4 percent of a lubricating agent and 0.5-1.5 percent of a flavoring agent, wherein the filler is at least two of microcrystalline cellulose, pre-gelatinized starch, lactose and mannite; the disintegrant is cross-linked sodiumcarboxymethylcellulose and/or cross-linked polyvidone; the bonding agent is polyvidone K30; the surfactant is sodium dodecyl sulfate; the lubricating agent is magnesium stearate and superfine silica gel powder; and the flavoring agent is aspartame and steviosin. The invention further provides a preparation method of the dispersing tablet. The preparation method is easy and convenient to operate, has low cost, and is suitable for industrial production. An obtained product has stable and controllable quality, attractive appearance, good mouthfeel and proper hardness, is fully disintegrated in water at the temperature of 20+/-1 DEG C within 3 minutes, and passes through a No.2 sieve; and the medicament dissolvability is over 85 percent 30 minutes later.
WO2009135959A1 Food product for enterally or orally feeding diabetic patients The invention relates to a food product for enterally or orally feeding a diabetic patient, said product comprising a proteinic mixture (23% of the total energy) based on caseinate, pea protein and milk serum proteins, a lipidic mixture (45% of the total energy) based on vegetable oils and purified fish oil, and a mixture of carbohydrates with a low glycemic index (32 % of the total energy), comprising type IV resistant starch, maltodextrin 5-8 DE, inulin and cellulose and vitamines and minerals.
CN102304162A Fullerene galactoside derivative, and preparation method and application thereof The invention relates to a new polymer compound, namely a fullerene galactoside derivative, which is a fullerene mono- and/or bis-addition acetylated galactoside. The invention also relates to a preparation method for the fullerene galactoside derivative, and application of the fullerene galactoside derivative in removal of free radicals. The fullerene galactoside derivative can make the auto-oxidation rate of pyrogallol reduced, which indicates that the derivative has the capacity of removing super oxygen negative ion free radicals, is a good antioxidant, and is widely applied to the fields of biomedicines and cosmetics.
US20100008985 Dosage unit for sublingual, buccal or oral administration of water-insoluble pharmaceutically active substances One aspect of the invention relates to a pharmaceutical dosage unit for sublingual, buccal, pulmonary or oral administration, said dosage unit having a weight of 20-500 mg and comprising 1-80 Wt. % of a microgranulate that is distributed throughout a solid hydrophilic matrix; said microgranulate being characterised in that it: has a volume weighted average diameter of 5-100 m; contains at least 0.01 wt. %, preferably at least 0.1 wt. % of one or more water-insoluble pharmaceutically active substances; contains at least 10 wt. %, preferably at least 20 wt. % of an emulsifier component; and is capable of forming a micro-emulsion upon contact with saliva or water. The dosage units of the present invention achieve the inherent benefits of oral delivery whilst at the same time realising a high transmucosal absorption rate of the cannabinoids contained therein. Other aspects of the present invention relate to the use of the aforementioned dosage units in the therapeutic or prophylactic treatment and to a process for the manufacture of said dosage units.
US20090068178 Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin The present invention is directed to compositions of matter useful for the treatment of hematopoietic tumor in mammals and to methods of using those compositions of matter for the same.
WO2013025984A2 Cannabinoid receptor treatments The present invention includes methods and compositions for treating a transplant recipient by administration of a CB2 receptor agonist either alone or in combination with one or more active pharmaceutical ingredients to block the rejection of foreign tissue and prolong grafted organs, tissues and cells.
EP2093292A2 Inhibition of specific histone deacetylase isoforms This invention relates to the inhibition of histone deacetylase expression and enzymatic activity. The invention provides methods and reagents for inhibiting specific histone deacetylase (HDAC) isoforms by inhibiting expression at the nucleic acid level or enzymatic activity at the protein level.
EP1265867B1 Malonic acid derivates, processes for their preparation, their use as inhibitor of factor xa activity and pharmaceutical compositions containing them The present invention relates to new compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula (I), wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of the formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula (I) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I), in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and auxiliary substances.
EP2010504A1 Quinazolin-4-one derivatives, process for their preparation and pharmaceutical compositions containing them The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
US6998422 Using pravastatin mixture with taurine, panthethine and inosiutol and hexanicotinate; anticholesterol agent, cardiovascular disorders Compositions having excellent blood lipid peroxide lowering activity are provided. In particular, compositions for lowering lipid peroxides in the blood which contain pravastatin together with at least one substance selected from the group consisting of taurine, pantethine and inositol hexanicotinate. Use of these compositions enables the provision of excellent preventive or remedial agents capable of lowering the concentration of lipid peroxides in the blood which show effects of injuring vascular endothelial cells, accelerating platelet aggregation, forming foam cells, etc.
WO2010104023A1 Infusion solution for administration to peripheral vein comprising carbohydrate solution having vitamin b1 contained therein stably Disclosed is an infusion solution for the administration to a peripheral vein, which comprises a carbohydrate solution and an amino acid solution, wherein the carbohydrate solution and the amino acid solution are contained in a dual chamber container separately. In the infusion solution, N-acetylcysteine is added to the carbohydrate solution containing vitamin B1 to stabilize vitamin B1.
US20050065118 Compound containing 1,3,4-thiadiazole group; anticancer agents; autoimmune disease; antidiabetic agents Organosulfur modulators of tyrosine phosphatases and their use in the treatment of disease are disclosed.
US20100216830 Oral Composition Comprising A Cooling Agent The present invention relates to a formulation comprising an endothermic cooling agent selected from the group consisting of xylitol, sorbitol, mannitol and erythritol having a heat of enthalpy between −10 cal/g and −100 cal/g, and one or more active agents wherein the endothermic agent is present in the formulation at an amount less than 10% w/w.
WO2007005176A1 Pyrrolidinones for the treatment of glaucoma and ocular hypertension Disclosed herein is a compound comprising Formula (I) or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, X, R and D are as described. Methods, compositions, and medicaments for the treatment of glaucoma and ocular hypertension are also disclosed.
CN101732280A Oral preparation of novel colonic positioning release medicine The invention discloses an oral preparation of a colonic positioning release medicine, which is formed in such a way that the effective component of olsalazine sodium and a medicinal carrier form a medicine tablet core together, the outside of the medicine tablet core is wrapt with isolation layer coating liquid comprising an imbibition type high molecular material, and the outermost layer of the medicine tablet core is wrapt with colonic dissolvable coating liquid containing a colonic dissolvable type high molecular material, wherein the weight ratio of the medicine tablet core to the isolation layer coating liquid to the colonic dissolvable coating liquid is 1:0.2-1.2:0.5-2. The olsalazine sodium colonic positioning enteric coated tablet avoids the first pass effect of the medicine, avoids stimulating the stomach and the small intestine, enables a coating to be dissolved according to the condition of high pH at the tail end of the small intestine and the position of the colon and acts as the function of colonic positioning release. In the invention, an azo bond is ruptured under the function of colonic bacteria and is split into 5-aminosalicylic acid with 2 molecules, thereby achieving the function of suppressing an inflammatory reaction and diarrhea.
CN101007814A Pyrrolehexa-heterocyclic compound and pharmaceutical use thereof The invention relates to pyrrolo six-member heterocyclic compounds with a general formula (I) and pharmaceutically acceptable salts, wherein the substituent groups in the general formula are defined in descriptions, as well as compositions containing the derivative. The invention also relates to the process for preparing the compound and the use in preparing protease inhibitor.
CN102488699A Application of paeoniflorin in preparation of medicine for preventing and curing pulmonary fibrosis The invention relates to the field of medicine, in particular to application of paeoniflorin in preparation of medicine for preventing and curing pulmonary fibrosis. A mouse pulmonary fibrosis model is copied through dripping bleomycin in a trachea, the influence of the paeoniflorin on changes of mouse pulmonary pathology and related indicators is researched, the function of preventing the pulmonary fibrosis of the paeoniflorin is proved, and a basis is provided for using the paeoniflorin to prepare the medicine for preventing and curing the pulmonary fibrosis.
CN101921256A Diphenyl pyrone amide derivative and preparation method and application thereof The invention discloses a diphenyl pyrone amide derivative with the following general formula and a preparation method thereof, n in the formula is 1 or 2, R is heterocyclic radical and substituted heterocyclic radical or R1 and R2 are alkyl. The diphenyl pyrone amide derivative has the role of in vitro inhibition of acetylcholine esterase and can be used for preparing drugs for treating presenile dementia.
CA2283326C An aqueous metal bicarbonate solution and method of use An aqueous neutral to mildly alkaline metal bicarbonate solution is disclosed. The solution comprises metal bicarbonate dissolved in the solution, the metal bicarbonate comprising bicarbonate anions and metal cations. In addition there is a pH adjusting agent in the solution in an amount whereby the solution is at a neutral to mildly alkaline pH. Also disclosed is a process of preparing an aqueous neutral to mildly alkaline metal bicarbonate solution comprising bicarbonate anions and metal cations. The process comprises reacting a compound selected from the group consisting of metal carbonate, metal carbonate hydroxide, metal oxide, metal hydroxide and any mixture thereof with an effective concentration of a pH adjusting agent to produce the aqueous neutral to mildly alkaline metal bicarbonate solution, wherein the pH adjusting agent is present in an amount whereby the solution is at a neutral to mildly alkaline pH. Further disclosed are a method of preventing and/or treating certain inflammatory diseases and/or degenerative diseases in a mammal, a method of preventing and/or treating certain viral diseases in a mammal, a method of decreasing and/or treating senescence and/or of increasing longevity in a mammal, a method of scavenging protons in a mammal, a method of decreasing proton concentrations in a mammal by altering carbonic anhydrase enzyme reactions in said mammal, a method of decreasing inflammation and/or inflammatory conditions in a mammal and a method of increasing motor activity and/or decreasing fatigue in a mammal.
CN102441030A Compound medicine for treating fungus infection diseases, its preparation method and quality control technology The invention discloses a compound medicine for treating fungus infection diseases, such as tinea corporis, tinea cruris, tinea manuum, tinea pedis, tinea versicolor, tinea capitis, candidal paronychia and candidal vulvovaginitis, and a preparation method and a quality control technology of the compound medicine. The compound medicine comprises cortex kadsurae radicis, benzoic acid, salicylic acid, golden larch bark, clotrimazole, diphenhydramine hydrochloride, and peppermint oil. The compound medicine can be prepared into a solution, a paste agent and a gel. The solution of the compound medicine are prepared by the following steps: taking cortex kadsurae radicis and golden larch bark and cutting into strips (3-5 mm), adding ethanol having a certain concentration to soak for 7 days, stirring, filtering, washing filter residues with a little 70 % ethanol, combining the filtrates, adding benzoic acid and the like for dissolving, adding 70 % ethanol to 90 % of a total concentration, adding distilled water to the total concentration. The quality control technology of the compound medicine defines a content measurment method of benzoic acid, salicylic acid, clotrimazole, and diphenhydramine hydrochloride. The compound medicine has the advantages of definite therapeutic effect, fast effect taking, fundamental control of diseases, little side effect and the like.
US20120225893 Combination of an antipsychotic and an anti-inflammatory agent The present invention relates to a pharmaceutical composition comprising an antipsychotic in combination with an anti-inflammatory agent, and to the use thereof in the treatment of psychotic disorder, and in particular, of schizophrenia.
CN101921269A Method for preparing HCV (Hepatitis C Virus) inhibitor The invention discloses a method for preparing an HCV (Hepatitis C Virus) inhibitor. The method comprises the following steps of: (1) obtaining a compound of a formula (6) through diazotizing, hydrolyzing, etherifying, reducing and acylating by using a 3-nitroaniline compound as a raw material; (2) providing a compound of a formula (10); (3) condensing and cyclizing the compound of the formula (10) and the compound of the formula (6) to prepare a compound of a formula (12); and etherifying and cyclizing the compound of the formula (12) and a compound of a formula (13) to obtain an HCV inhibitor of a formula A. The method has the advantages of easy raw material obtaining, low price, moderate reaction condition, simple operation and easy industrialization.
CN101659663B Indolizine derivative as well as preparation method and application thereof The invention discloses an indolizine derivative as well as a preparation method and an application thereof, which belongs to the technical field of medicinal chemistry. The preparation method of the indolizine derivative is characterized by comprising the steps of: dissolving 10mmol of onium salt in 40mL of DMF; adding 2mL of triethylamine, 40mmol of acrylontitrile, and 4g of TPCD; reacting for 4 to 15 hours at the temperature of 70 to 120 DEG C; cooling; pouring the reactant into 100mlL of 5 percent hydrochloric acid liquid; separating out sediment; filtering to obtain a crude product; and chromatographing through silicagel column to obtain the product. The invention creatively designs to induce a cyclopropyl group with unique bioactivity into an indolizine system and the compounded indolizine derivatives have good activity for resisting the increment of liver cancer cell strain (Hep-G2); and the indolizine derivatives can be further modified to serve as new anti-liver cancer medicine.
US20110200686 Compositions of modulators of the wnt/b-catenin pathway and an n-cinnamyl-n'benzhydryl piperazine and their use in treating neoplastic conditions including malignant melanoma The present invention is directed to a composition comprising a modulator of the Wnt/β-catenin pathway or a pharmaceutically acceptable salt thereof and an N-cinnamyl-N′-benzhydryl piperazine or a pharmaceutically acceptable salt thereof. The present invention is also directed to a method of treating a neoplastic condition in a subject by administering the modulator of the Wnt/βcatenin pathway or a pharmaceutically acceptable salt thereof and an N-cinnamyl-N′-benzhydryl piperazine or a pharmaceutically acceptable salt thereof to the subject under conditions effective to treat a neoplastic disorder.
US20080193479 Method and Compositions for the Treatment of Hematologic Cancers The present invention relates to oncolytic Picornaviruses and methods and compositions for treating subjects having hematologic cancers. These include methods and compositions for treatment of myeloma, using disclosed Picornavirus such as Coxsackievirus, in methods of direct or indirect administration to subjects and ex vivo purging of malignant cells within auto grafts prior to transplantation.
US20090098177 Methods and devices for tissue repair Methods for treating diseased or damaged tissue in a subject are disclosed, involving administering to said subject at a site wherein diseased or damaged tissue occurs, cells of a type(s) normally found in healthy tissue corresponding to the diseased or damaged tissue, and/or suitable progenitor cells thereof, in association with bioresorbable beads or particles and optionally a gel and/or gel-forming substance. Where the cells an/or suitable progenitor cells thereof are chondrocytes, embryonic stem cells and/or bone marrow stromal cells, the methods of the invention are suitable for treating, for example, articular cartilage degeneration associated with primary osteoarthritis. Also disclosed is a device having tissue-like characteristics for treating diseased or damaged tissue in a subject, wherein the device comprises cells of a type(s) normally found in healthy tissue corresponding to the diseased or damaged tissue, and/or suitable progenitor cells thereof, in association with bioresorbable beads or particles and optionally a gel and/or gel-forming substance.
EP2101806A2 Treatment of disease or injury of the nervous system using agents that decrease the activity of the melanocortin 4 receptor Novel methods are provided for modulating CNS cell neogenesis in the CNS cells in vitro or in vivo, involving the use of agents that decrease the activity of the melanocortin 4 receptor (MC4R). When the methods of the invention are applied to a subject such as a human, it may be used for reducing a symptom of a CNS disorder.
US7687476 administering 4-thiouridine, isomaltitol and uridine as antiinflammatory agents and/or problems in hemostasis related to platelet function The present invention relates to the use of one or more of the compounds of the group consisting of 4-thiouridine, isomaltitol, and uridine in the preparation of therapeutically effective compositions against acute or chronic inflammations, and/or problems in hemostasis related to platelet function, as well as a method for treatment of acute or chronic inflammations, and/or problems in hemostasis related to platelet function with the exception of the use of uridine in the treatment of inflammatory conditions caused by a bacterial infection.
US20100234294 Identification of new isoforms of the mhc-class i specific receptor cd160 and uses thereof The present invention concerns an isolated polypeptide comprising a sequence selected in the group comprising SEQ ID NO.7, its orthologs, and derivatives thereof; a polynucleotide comprising a nucleic acid sequence encoding for said polypeptide; a vector comprising said polynucleotide; a host cell genetically engineered with said polynucleotide or with said vector; a pharmaceutical composition comprising said polypeptide, a polynucleotide coding for said polypeptide or a vector comprising said polynucleotide, and optionally a pharmaceutically acceptable carrier; a method for screening for antagonists and/or agonists of said polypeptide; and uses of said polypeptide, a polynucleotide coding for said polypeptide or a vector comprising said polynucleotide, for the manufacture of a medicament.
US20120276072 Constructs for expressing lysosomal polypeptides Provided are isolated nucleic acids for expressing lysosomal polypeptides such as lysosomal acid α-glucosidase (GAA) and vectors comprising the same. The invention provides an isolated nucleic acid encoding a chimeric polypeptide comprising a secretory signal sequence operably linked to a lysosomal polypeptide. The invention also provides an isolated nucleic acid comprising a coding region encoding a GAA and a GAA 3′ untranslated region (UTR), wherein the GAA 3′ UTR comprises a deletion therein. The invention further provides an isolated nucleic acid comprising a coding region encoding a GAA and a 3′ UTR wherein the 3′ UTR is less than about 200 nucleotides in length and comprises a segment that is heterologous to the GAA coding region. Also provided are methods of making and using delivery vectors encoding lysosomal polypeptides to produce the lysosomal polypeptide to treat subjects afflicted with a deficiency in the lysosomal polypeptide.
EP1414467B1 Topical treatment for mastalgia The invention relates to a composition for medical treatment by topical application. In addition to the usual components of topical forms of application, the inventive composition contains an aromatase inhibitor. The active agent or the composition containing this active agent is particularly suitable for the prevention and treatment by therapy of mastalgia.
US20130085172 Crystalline forms of a 3-[2-methanesulfonyl-1-(4-trifluoromethyl-phenoxy)ethyl]pyrrolidine compound The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.
WO2014020608A1 Methods of diagnosing and treating motor neuron diseases A method of treating a motor neuron disease (MND) in a subject in need thereof is provided. The method comprising administering to the subject a therapeutically effective amount of an agent capable of enhancing processing of a pre-mi RNA, thereby treating the MND in the subject.
WO2013068971A2 Cosmetic composition comprising a modified alpha-alkoxysilane The invention relates to a cosmetic composition, in particular a composition for making up and/or caring for keratin materials, preferably a nail makeup, comprising the compound of chemical formula (I) below: (I) in which: a and b independently represent an integer between 0 and 20; R1, R2, R11 and R12 independently represent an ethoxy group, a group (Ci-C2o)alkyl optionally substituted with an amino group; R3, R4, R5, R6, R7, R8, R9 and R1O independently represent a hydrogen atom or a group (C1-C10)alkyl; XI and X2 independently represent a carboxyl, carbamate, amide, carbonate, ureido or sulfonate group, an oxygen atom or a NH group; Y represents a hydrocarbon-based group comprising from 2 to 800 carbon atoms, the said hydrocarbon-based group being a linear or branched divalent group, bearing one or more aromatic or non-aromatic rings. The invention also relates to a cosmetic process, characterized in that it comprises at least one step which consists in applying a cosmetic composition as above defined to keratin materials.
WO2012095804A1 Means for reducing or eradicating the tumour capacity of cancer stem cells and/or metastatic stem cells. The subject matter of the invention is molecules with anti-protease activity for preferentially targeting, in a tumour, the population of cancer stem cells, or CSCs, and/or the metastatic stem cells, expressing embryonic stem cell markers, including Oct-4 and/or Nanog and/or Sox2, defining an embryonic signature in order to reduce the tumour or metastatic capacity of said population, or even to eradicate same. (No figure to be published).
US20100034887 Bursting Pellets In the present invention, a new pharmaceutical formulation of bursting pellets comprising in the core a high dose of a low potency active substance which is poorly soluble in water is described. Release of the active substance from the core takes place within minutes.
WO2005115369A2 Use of ppar agonists to treat ruminants The use of a PPAR agonist in the manufacture of a medicament to increase ruminant serum glucose concentrations, and preferably, the use for the palliative, prophylactic or curative treatment of ruminant disease associated with reduced serum glucose concentration. The ruminant disease associated with reduced serum glucose concentration includes fatty liver syndrome, dystocia, immune dysfunction, impaired immune function, toxif ication, primary ketosis, secondary ketosis, downer cow syndrome, indigestion, inappetence, retained placenta, displaced abomasum, mastitis, (endo-) -metritis, infertility, low fertility, lameness, subacute rumen acidosis and inadequate nutrient intake associated with stress e.g. heat, poor housing, overcrowding, shipping, dominance or illness, and to increase milk quality and yield.
US7196086 Substituted dihydroquinazolines The invention relates to substituted dihydroquinazolines and to processes for their preparation and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for use as antiviral agents, in particular against cytomegalo viruses.
US20140107047 Cosmetic compositions for increasing bioavailability of active compounds Aqueous compositions comprising a) at least one active compound and b) at least one hydrotrope in an amount effective to increase transdermal penetration of the active compound, and methods for increasing bioavailability of active compounds are provided.
EP2444411A1 Tripeptide boronic acid or boronic ester, preparative method and use thereof The present invention discloses proteasome inhibitors of tripeptide boronic acids or boronic esters represented by Formula (I), preparative method and use thereof. The proteasome inhibitors are therapeutical agents for treating malignant tumor, various nervous system degenerative diseases, muscle cachexia or diabetes, wherein the malignant tumor is leukemia, gastric cancer, hepatocarcinoma or nasopharyngeal carcinoma.
US20050031706 A bismuth containing agent , a non-clay-derived suspending agent; an stabilizer for reducing viscosity change during storage of the formulation and water The present invention provides a pharmaceutical composition comprising at least one pharmaceutically acceptable bismuth-containing compound, at least one pharmaceutically acceptable non-clay-derived suspending agent, water, and a stabilizing means for reducing viscosity change upon storage of the composition. The suspension exhibits reduced change in viscosity by comparison with an otherwise similar suspension excepting the stabilizing means. Such compositions are useful in the prevention and treatment of gastrointestinal diseases and/or disorders.
US20050079176 Treating stress response with chemokine receptor ccr5 modulators The use of chemokine receptor CCR5 modulators (e.g., CCR5 antagonists) is disclosed for the treatment or prevention of stress response (e.g., fever) in a subject resulting from surgery, infection or other insult to the subject (e.g., a warm-blooded vertebrate). Methods for treating or preventing disorders involving the activation of pro-inflammatory cytokines by administration of a CCR5 modulator, for inhibiting the endogenous production of pro-inflammatory cytokines by the administration of CCR5 modulators, and for determining the efficacy of CCR5 modulators in correcting abnormal levels of pro-inflammatory cytokines are also disclosed.
CN102697834A Bottle gourd essence lotion The invention discloses a bottle gourd essence lotion, which comprises the following components in weight percentage: 80-95 percent of purely natural and fresh collected bottle gourd lotion and 5-20 percent of coarse salt (iodine-containing low-sodium coarse-particle salt), wherein the weight percentage of the coarse salt is 5-10 percent preferably, the sum of the weight percentage of all the components is 100 percent, and the pH value is 7.5-8.0. The bottle gourd lotion is reasonable in structure and good in health-care effect, can be easily processed and manufactured, has no toxic and side effects after being used for a long time, is safe and reliable and can be used for reducing the dependence on other hormone drugs. By often using the bottle gourd essence lotion, a pretty good anti-inflammation and antipruritic effect can be performed on facial acnes, whelks, skin itching, crissum itching and external genitalia itching which are caused by seasonal variations, piles, nameless pyogenic infections and pimples and galls caused by getting angry. Meanwhile, a very good anti-inflammation, antipruritic and analgesic effect can be performed on burn itching, scald itching, cut itching, finger seam peeling itching, nail seam peeling itching, dermatophytosis itching, sandworm foot peeling and dampness itching, whereas scars are not left. Proved by practice, the bottle gourd essence lotion is most efficient on symptoms, such as the acnes, the whelks and the pimples and galls by using a method of massage combined with face towel wet compressing, and the bottle gourd essence lotion can take effect after being used for 5-7 times a day. Moreover, the bottle gourd essence lotion is good in use feeling and convenient in carrying and use and can be widely used for human body health care and daily life.
US20110223230 Hydrogel formulations A polymeric prodrug composition including a hydrogel, a biologically active moiety and a reversible prodrug linker. The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on its surface. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety.
US20110189259 Multidirectional mucosal delivery devices and methods of use The present invention relates to a pharmaceutical dosage form for transmucosal delivery of an active agent to two or more mucosal surfaces. The dosage form is presented as a transmucosal delivery device. The devices of the invention may include at least two mucoadhesive surfaces. The devices may further include an intermediate layer disposed between the mucoadhesive layers. The pharmaceutical can be incorporated in any one or all of the mucoadhesive layers or the intermediate layer. Upon application, the device adheres to at least two surfaces, providing transmucosal delivery of the drug to at least two surfaces.
US20080020965 Oxidative damage and protease activity resistance; catalytic efficiency; deep vein thrombosis, disseminated intravascular coagulation, acute coronary syndrome; targeting protein, that interacts with tissue factor or the factor VIIa/tissue factor complex This invention relates to novel fusion proteins which are comprised of a targeting protein that binds tissue factor (TF), which is operably linked to the thrombomodulin (TM) EGF456 domain alone or in combination with at least one other TM domain selected from the group consisting of the N-terminal hydrophobic region domain, the EGF123 domain, the interdomain loop between EGF3 and EGF4, and the O-glycosylated Ser/Thr-rich domain, or analogs, fragments, derivatives or variants thereof. The fusion protein binds at the site of injury and prevents the initiation of thrombosis. The fusion protein can be used to treat a variety of thrombotic conditions including but not limited to deep vein thrombosis, disseminated intravascular coagulation, and acute coronary syndrome.
CA2150185C Pharmaceutical composition for the treatment of stoma-peripheral inflammation The disclosure describes a method of treating a patient suffering from stoma-peripheral inflammation diseases, comprising orally administering to said patient an effective amount of a pharmaceutical composition in dosage unit form comprising a spherical activated carbon having a particle size of 0.05 to 2 mm.
WO2006090853A1 Nitrogenous heterocyclic compound and medicinal use thereof A compound represented by the general formula (I): (I) (wherein the symbols are the same as defined in the description), a salt thereof, an N-oxide form or solvate of either, or a prodrug of any of these. The compound represented by the general formula (I) has CXCR4 antagonistic activity. It is hence useful as, e.g., a preventive and/or therapeutic agent for CXCR4-mediated diseases such as inflammatory/immunologic diseases (e.g., articular rheumatism, arthritis, retinopathy, pulmonary fibrosis, and rejection reactions of transplanted organs), allergic diseases, infectious diseases (e.g., human immunodeficiency virus infection and acquired immunologic deficiency syndrome), psychoneurotic diseases, cerebral diseases, cardiac/vascular diseases, metabolic diseases, cancer diseases (e.g., cancer and cancer metastasis) or as a drug for regenerative medical.
CN1615846A Soft capsule containing bergenin and its preparing method The soft bergenin capsule has raised bergenin stability, raised bergenin leaching degree and bioavailability. The soft bergenin capsule contains bergenin as active component in 10-300 mg/capsule, preferably 62.5-250 mg/capsule, nonunion 1-4 mg, solvent and diluent in 50-60 %, emulsifying co-solvent in 5-10 % and antioxidant stabilizer in 2-7 %. The capsule shell is prepared with gelatin, glycerin, sorbic alcohol, etc. and has titania in the amount of 0.5-0.7 % of gelatin weight added as the shading agent.
EP1839643A1 Cosmetic and pharmaceutical foam carrier The invention provides a quick-break, alcohol-free, cosmetic and pharmaceutical foam carrier comprising about 20%-60% hydrophobic volatile solvent, about 20%-60% water, about 3%-20% of polyol, and about 0.1%-7.5% of a surface active agent.
WO2008053920A1 Physiologically active substance-containing granular composition and method of producing the same It is intended to provide a granular composition comprising an oily component (A), which contains a hardly water-soluble physiologically active substance and is polydispersed while forming domains in a matrix made of a water-soluble filler having a water-soluble polymer as the main component, having a spherical degree of 0.9 or more and being excellent in solubility in water, workability, tabletting properties and heat stability; and a method of producing the same. It is also intended to provide a food, a food with nutrient function claims, a food for specified health uses, a nutritional supplement, a nutrient, a drug for animals, a drink, a feed, a pet food, a cosmetic, a drug, a remedy, a therapeutic and so on each containing the granular composition as described above.
US20090068174 Therapeutic alkaline protease compositions and use in facilitating the transport of agents across the gastrointestinal mucosal lining A method of treating an inflammatory condition involving TNF-α in a mammal by administering to a patient a composition with an effective amount of an isolated alkaline protease in an amount effective to inactive TNF-α. The invention also involves compositions, including pharmaceutical compositions containing an isolated alkaline protease in an amount effective to inactive TNF-α especially those from Aspergillus oryzae and/or serve as a transepithial carrier.
US7071177 P-(sulfonyl) aryl and heteroarylamines as anti-inflammatory agents This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
CN103536697A Nutrient solution capable of increasing fertilization rate of artificial poultry insemination The invention discloses a nutrient solution capable of increasing the fertilization rate of the artificial poultry insemination, relating to the technical field of poultry propagation. The nutrient solution comprises the following materials: Chinese angelica, radix paeoniae alba, rehmannia glutinosa, astragalus membranaceus, teasel roots, ligusticum wallichii, liquorice, fructus aurantii and amino acids. The method comprises the following steps: A. preparing the materials, namely respectively weighing the materials by weight parts for standby use; b. soaking, namely placing the materials in a container, adding 40-60 parts of water in the container by weight parts, and soaking for 0.5-1h; C. distilling, namely placing soaked materials and soaking water in a distilling device together, distilling, and collecting 1-3 parts of distilled distilling liquid, so as to obtain the nutrient solution capable of increasing the fertilization rate of the artificial poultry insemination. The nutrient solution has the effects of replenishing energy, enhancing the fatigue resistance, slowing down the natural aging, adjusting the body immunity, resisting the irradiation, resisting bacteria, diminishing the inflammation and the like, can be used in the artificial poultry insemination breeding process, has the characteristics of increasing the fertilization rate and the like, not only can be used for the breeding of chickens and also can be used for breeding ducks or geese.
EP1307187B1 Use of 13-cis retinoic acid for the treatment of emphysema The invention relates to the use of 13-cis-retinoic acid, pharmaceutical compositions of 13-cis-retinoic acid for the treatment of emphysema, to methods of treating emphysema with 13-cis-retinoic acid, pharmaceutical compositions of 13-cis-retinoic acid useful in the treatment of emphysema and methods for delivering formulations of 13-cis-retinoic acid to the lung of a mammal suffering form emphysema.
US20080161281 Amino-Substituted Tricyclic Derivatives and Methods of Use Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.
WO2009083268A2 17-(1'-propenyl)-17-3'-oxidoestra-4-en-3-one derivative, use thereof, and medicament containing said derivative The invention relates to 17-(1'-propenyl)-17-3'-oxidoestra-4-en-3-one derivatives with general chemical formula (1) wherein the radicals Z, R4, R6a, R6b, R7, R15, R16a, R16b and R18 have the designations given in claim 1, and to the solvates, hydrates and salts thereof, including all stereoisomers of said compounds. The invention also relates to the use of said derivatives for producing a medicament for oral contraception and for the treatment of premenopausal, perimenopausal and postmenopausal complaints, and medicaments containing said derivatives, especially the application thereof in the cited cases. The derivatives according to the invention have a gestagenic effect, and in preferred cases, also an anti-mineral corticoidal and neutral to lightly androgenous effect.
US20120244221 Extended-release formulation for reducing the frequency of urination and method of use thereof Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.
EP2014670A2 Production of Glucosinolates from Agricultural By-Products and Waste The present invention relates to a process for producing glucosinolates, particularly glucoraphanin, from cruciferous plants. More particularly, a method is provided for producing glucosinolates from agricultural by-products and waste. The general method comprises providing a mixture of glucosinolate-containing plant material and liquid, heating the mixture to inactivate enzymes in the plant material, contacting the heat inactivated mixture with an anion exchange membrane whereby at least a portion of the glucosinolates are extracted from the liquid and absorbed onto the anion exchange membrane, and releasing the glucosinolates from the anion exchange membrane. Preferably, the extraction and release steps are repeated at least once. The glucosinolates produced by the method of the invention may be incorporated into a variety of food products, pharmaceuticals, and health supplements.
CN102746326A P-nitro-cinnamic acid metal complex and preparation method and application thereof The invention belongs to the technical field of preparation of a cinnamic acid derivative, and particularly relates to a p-nitro-cinnamic acid metal complex and a preparation method and an application thereof. The complex is prepared by the following steps of: dissolving p-nitro-cinnamic acid into a sodium hydroxide solution; adding a sulfate aqueous solution of a transition group metal element to obtain a p-nitro-cinnamic acid metal salt; mixing the p-nitro-cinnamic acid metal salt with a diamine ammonia aqueous solution; adding a methanol solvent; and standing at the room temperature till methanol is volatilized completely to obtain the p-nitro-cinnamic acid metal complex, wherein the transition group metal element is copper, cobalt, cadmium, nickel or zinc. The p-nitro-cinnamic acid metal complex has high urease inhibitory activity and higher medicinal property, and can be used for preparing a urease inhibitor.
WO2014085284A1 Triazolo-pyrazine derivatives useful in the treatment of disorders of the central nervous system Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
WO2007138998A1 Pharmaceutical composition comprising nitrogenated fused cyclic compound Disclosed is a pharmaceutical composition which is effective for the treatment or prevention of a disease associated with uric acid, such as hyperuricemia, tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urinary calculus, renal dysfunction, coronary disorder and ischemic heart disease, and which has excellent long-term stability and elution properties (disintegration properties). The pharmaceutical composition comprises a nitrogenated fused cyclic compound represented by the general formula [1] or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable additive, wherein the nitrogenated fused cyclic compound or the pharmaceutically acceptable salt thereof is not contacted with a basic additive. [1] wherein each symbol is as defined in the description.
US20080103176 N-{1-(3,5-Difluoro-benzyl)-3-[7-(2,2-dimethyl-propyl)-2-piperidin-1-yl-1,2,3,4-tetrahydro-naphthalen-1-ylamino]-2-hydroxy-propyl}-acetamide; 13-secretase inhibitor; Alzheimer's disease; inhibitors of beta-secretase, that inhibit beta-secretase-mediated cleavage of amiloid precursor protein APP This invention is directed to compounds of the formula (I), as defined herein. The compound of formula I may be used, for example, to treat a disorder or condition that may be treated by inhibiting 13-secretase.
WO2011042890A2 Use of phenolic compounds for protein deglycolysation The invention relates to the use of at least one compound of the general formula (I): the physiologically acceptable salts, esters and derivatives thereof for inducing deglycolysation of condensed glycated proteins.
CN103720696A Preparation process for improving bioavailability of valsartan and hydrochlorothiazid capsules The invention belongs to the technical field of medicine preparation, and particularly relates to a preparation process for improving bioavailability of valsartan and hydrochlorothiazid capsules. The process provided by the invention comprises the following specific steps: 1) processing valsartan and hydrochlorothiazid by means of micronization, sieving a filler, a disintegrating agent, an adhesive and a solubilizer with a 80-mesh sieve, and sieving a lubricating agent with a 40-mesh sieve for later use; 2) weighing a prescribed dose of the valsartan, the hydrochlorothiazid, the filler, the disintegrating agent, the adhesive and the solubilizer, and uniformly mixing in a high-speed mixing granulator; 3) granulating the uniformly-mixed powder by using a dry type granulator, adding a prescribed dose of the lubricating agent for strengthening granules and then uniformly mixing the lubricating agent with the powder; 4) filling capsules. Compared with the prior art, the preparation process for improving the bioavailability of valsartan and hydrochlorothiazid capsules can improve the dissolution rate and increase the solubility by processing the raw materials by means of micronization, adding special auxiliary materials and adopting dry granulation, thus the bioavailability of the valsartan and hydrochlorothiazid capsules is improved.
EP2268290A2 Styrene maleic anhydride based formulation for male contraception and prostate cancer The invention provides a styrene maleic anhydride based synergistic formulation comprising styrene maleic anhydride [SMA] having lower molecular weight and styrene maleic anhydride [SMA] having higher molecular weight dissolved in DMSO, and being capable of preventing the prostate cancer as well as causing male contraception even when administered in smaller doses for one or two administrations in the life time and predominantly causing no or minimal side effects, and still being reasonably affordable by common man, and the formulation being capable of traveling along the vas deferens after causing male contraception in the vas deferens to the prostate gland and getting absorbed into the epithelial zone of the prostate gland.
US20090069383 Thrombin Receptor Antagonists A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.
CN103301104A Use of danshinolic acid A composition in preparing ischemic penumbra treatment medicaments The invention relates to use of danshinolic acid A composition in preparing ischemic penumbra treatment medicaments. The composition is composed of danshinolic acid A, alkannic acid, rosmarinic acid, danshinolic acid B and danshinolic acid C, wherein the composition is prepared in the following weight ratios: 90-99% of danshinolic acid A, 0.1-3% of alkannic acid, 0.1-3% of rosmarinic acid, 0.1-3% of danshinolic acid B and 0.1-5% of danshinolic acid C.
WO2007006732A1 Synergistic combination for the treatment of pain (cannabioid receptor agonist and opiod receptor agonist) The invention relates to a pharmaceutical dosage form comprising an analgesic combination for simultaneous or sequential use which comprises a peripherally restricted cannabinoid CB1 receptor agonist having a brain Cmax to plasma Cmax ratio of less than 0.1 and an opioid receptor agonist, as well as to a method for treating pain using said pharmaceutical dosage form.
CN1923827A Eremophilone lactones acid natural product and application thereof The invention discloses an eremophilane lactone compound with chemical name as 3beta-chiretta acyloxy group-eremophile-7(11)-alkylene-12, 8beta-lactone-14-acid, which can inhibit the biological activity of HL-60, CNE, KB, Hela and P338D1.
US20080248055 Using glutamate decarboxylase therapeutic for treatment and prevention of pancreatic disorders The present invention regards methods and formulations for the treatment of diabetes and the prevention of autoimmune diabetes. The invention includes the administration of human recombinant GAD65 protein in a pharmaceutically acceptable adjuvant.
WO2013038259A1 Benzothiazinone derivatives as anti -tuberculosis agents Novel benzothiazinone derivatives of formula (I) or pharmaceutically acceptable salts or solvates thereof have been found to be effective against Mycobacterium tuberculosis strains and may thus be useful in the treatment of tuberculosis: wherein EWG (electron withdrawing group) = NO2, CN, CF3, F, Cl, Br, OCF3, OH, OR, OCHF2, COOR, wherein R is hydrogen or a straight or branched C1-C4 alkyl group, X = a bond or a straight or branched C1-C4 alkylene group which may be substituted with a group selected from F, Cl, Br, I or C1-C4 alkoxy; Y = hydrogen, a straight or branched C1-C4 alkyl group, OH or OR, wherein R is hydrogen or a straight or branched C1-C4 alkyl group; n = 0, 1 or 2; R1, R2 = hydrogen or substituent (s) which may be the same or different from each other and are selected from the group consisting of D, F, Cl, Br, CF3, a straight or branched C1-C4 alkyl group, a phenyl group, OR, SR, NR3R4, wherein R, R3, R4 may be the same or different from each other and are hydrogen or a straight or branched C1-C4 alkyl group or a phenyl group.
WO2011054811A1 Rna antagonists targeting hsp27 combination therapy The present invention relates to antisense oligomers targeting HSP-27 for the treatment of cancer in combination with a cytotoxic agent, such as TNF-alpha.
WO2012054698A1 Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt Provided herein are (8S, 9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-lH-1,2,4-triazol-5- yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fiuoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H- pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H- pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer.
EP1333841B1 M. tuberculosis chaperonin 10 and uses thereof The invention relates to the use of cpn 10 from Mycobacterium tuberculosis , or functionally equivalent molecules of fragments thereof, in the prevention and/or treatment of allergic conditions such as asthma, rhinitis/hay fever, eczema and anaphylaxis, which conditions are associated with an underlying Th2 cell over-reactivity, or cancerous conditions.
EP1011688B1 Use of uridine 5'-diphosphate and analogs thereof for the treatment of lung diseases Compounds of Formula (I) wherein X1 and X2 are each independently either O?- or S-; X¿3 and X4 are each independently either -H or -OH, with the proviso that X3 and X4 are not simultaneously -H; R1 is selected from the group consisting of O, imido, methylene and dihalomethylene; R2 is selected from the group consisting of H, halo, alkyl, substituted alkyl, alkoxyl, nitro and azido; R3 is selected from the group consisting of H, alkyl, acyl, aryl, and arylalkyl; and R4 is selected from the group consisting of -OR', -SR', -NR', and - NR'R'', wherein R' and R'' are independently selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, alkoxyl, and aryloxyl, with the proviso that R' is absent when R4 is double bonded from an oxygen or sulfur atom to the carbon at the 4-position of the pyrimidine ring, are used in methods of hydrating lung mucus secretions and treating lung disorders such as cystic fibrosis, ventilator-associated pneumonia, chronic bronchitis, chronic obstructive pulmonary disorder and primary ciliary dyskinesia. Pharmaceutical compositions containing compounds of Formula (I), and novel compounds of Formula (I) are also described.
US20110190252 Compositions including clavulanic acid and related methods of use Methods of treating a disorder in a subject comprising administering to a subject an elastase inhibitor such as clavulanic acid, sulbactam, or tazobactam are described.
CN102232075B Amino pyrazole compound The present invention provides amino pyrazole compounds useful in the treatment of chronic myeloproliferative disorders and various cancers, e.g., glioblastoma, breast cancer, multiple myeloma, prostate cancer, and leukemias.
CN102552206A Medicinal composition with anti-inflammatory and analgesic effects The invention which belongs to the technical field of medicines discloses a medicinal composition with anti-inflammatory and analgesic effects. The medicinal composition is characterized in that the medicinal composition comprises aceclofenac, a microcrystalline cellulose, pregelatinized starch, a hydroxypropyl cellulose, a lubricant and polyvinyl acetate phthalate; or the medicinal composition comprises aceclofenac, the microcrystalline cellulose, the pregelatinized starch, the hydroxypropyl cellulose, the lubricant, polyvinyl acetate phthalate and a polyacrylic resin III. The medicinal composition of the invention is determined through a disintegration test, a release degree test and the like, and medicinal preparations prepared from the medicinal composition of the invention have the excellent quality characteristics.
WO2011040070A1 Oral composition for alleviation of ultraviolet radiation-induced damage Disclosed are: an oral composition for alleviating ultraviolet radiation-induced damage, which can be used on a daily basis and is stable and safe; and a medicinal agent, an anti-wrinkle agent and a food composition, each of which comprises the oral composition. Specifically disclosed is an oral composition for alleviating ultraviolet radiation-induced damage, which comprises at least one compound selected from the group consisting of methionine and derivatives and/or salts thereof. The composition may be an anti-wrinkle agent, a pharmaceutical composition for treating and/or preventing skin diseases, a food composition, or a pharmaceutical composition for preventing or treating cataract. In the oral composition for alleviating ultraviolet radiation-induced damage, methionine may have a D-form.
CA2286091C Polymer-platinum compounds A polymer-platinum compound for use in tumor treatment is described. The compound is composed of a polymer backbone having platinum-containing side chains spaced along the polymer backbone. The side chains are composed of an oligopeptide attached at one end to the backbone and at the other end to the platinum compound.
CN102614144A Sodium rabeprazole medicinal composite and method for preparing same The invention discloses a sodium rabeprazole medicinal composite, which contains the active substances of sodium rabeprazole and stabilizing agent, wherein the weight ratio of the stabilizing agent and the sodium rabeprazole is 0.05-10/1, and the sodium rabeprazole medicinal composite also contains other optional pharmaceutically acceptable additives. The composite uses less amount of the stabilizing agent, has good stability and a simple preparing technology.
US6872407 Extended release formulations of erythromycin derivatives Disclosed is a pharmaceutical composition for extended release of an erythromycin derivative in the gastrointestinal environment. The composition comprises an erythromycin derivative and a pharmaceutically acceptable polymer so that, when ingested orally, the composition induces statistically significantly lower Cmax in the plasma than an immediate release composition of the erythromycin derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the erythromycin derivative upon multiple dosing. The compositions of the invention have an improved taste profile and reduced gastrointestinal side effects as compared to those for the immediate release composition.
US7695736 Powder of 30-90% a water-soluble cycloxygenase inhibitor, 5-60% of a buffer and 0-10% of other excipients A pharmaceutical composition comprises, in powder form, (a) at least one water-soluble therapeutic agent selected from selective COX-2 inhibitory drugs and prodrugs and salts thereof, for example parecoxib sodium, in a therapeutically effective total amount constituting about 30% to about 90% by weight, (b) a parenterally acceptable buffering agent in an amount of about 5% to about 60% by weight, and optionally (c) other parenterally acceptable excipient ingredients in a total amount not greater than about 10% by weight, of the composition. The composition is reconstitutable in a parenterally acceptable solvent liquid to form an injectable solution. A lyophilization process is provided for preparation of such a composition.
CN103656309A Auxiliary drug composition for bone fracture/bony crack healing The invention relates to auxiliary drug composition for bone fracture/bony crack healing. The auxiliary drug composition for bone fracture/bony crack healing is prepared by components in parts by weight as follows: 20-25 parts of sambucus chinensis, 15-20 parts of eupolyphaga, 15-20 parts of dragon's blood, 10-15 parts of reed roots, 8-13 parts of myrrh, 8-12 parts of semen strychni, 10-14 parts of native copper, 5-10 parts of crab meal, 5-10 parts of cutch, 6-9 parts of cinnabar, 6-9 parts of cucumber seeds, 5-7 parts of oysters and 3-5 parts of Chinese rice wine. The auxiliary drug composition is reasonable in compatibility, can rapidly take effect, has no side effects, is suitable for promoting repairing of bone breaking joints or cracks in the healing period of various bone fractures, bone cracks and traumatic injury, has a good therapeutic effect on long-time unhealed condition of comminuted fracture or bone breaking malposition after operation in hospital and has a certain curative effect on soft tissue injury, skin and flesh bruise caused by traumatic injury and lumbar spinal cord contusion.
CN103720676A Preparation method and application of novel oral ulcer antibacterial film The invention relates to a preparation method of a novel oral ulcer antibacterial film. The oral ulcer antibacterial film comprises, by weight: 1-20% of polyvinyl alcohol, 1-10% of polyacrylic acid, 0.5-5% of glycerol, 2-10% of water-soluble chitosan, 0.1-5% of bioactive glass, and the balance distilled water. The bioactive glass is evenly dispersed in the glycerol, and the bioactive glass and the glycerol are in a ratio of 1:0.5-1:2. Specifically, the bioactive glass comprises, by weight: 24.5% of CaO, 24.5% of NaO, 45% of SiO2, and 6% of P2O5. During preparation of the oral ulcer antibacterial film provided by the invention, under an aseptic condition, polyacrylic acid, polyvinyl alcohol, a mixed solution of bioactive glass and glycerol, and chitosan are added into distilled water in order, and during adding, the temperature, stirring time, complete dissolution and the pH value of the solution are controlled, thus finally obtaining a film-like material. The oral ulcer antibacterial film provided by the invention has good biocompatibility and degradability, and also has very good bacteriostatic and wound repair functions, thus being applicable to prevention and treatment of oral ulcer.
US20100280047 Salts of active ingredients with polymeric counter-ions Polymeric water-soluble salts of medicaments that are sparingly soluble in water, consisting of a polymer with anion character that is soluble in water at pH values of 2-13 and a sparingly soluble medicament with cation character.
CN102988579A Kidney-tonifying and bone-strengthening pill for preventing and treating osteoporosis The invention provides a kidney-tonifying and bone-strengthening pill for preventing and treating osteoporosis. The pill is prepared in the following steps: crushing the following components in parts by weight: 1 go 5 parts of achyranthes bidentata, 1 to 5 parts of red-rooted salvia root, and 4 to 6 parts of rehmannia; and uniformly mixing the drugs with 10 to 30 weight parts of chondroitin sulfate. The product has good effect of preventing and treating osteoporosis.
DE102006009889A1 Topical product, useful for the prevention of eye irritation, and for prevention and treatment of blepharitis, comprises cobalamin in the form of cyano-, hydroxy- and/or methyl-cobalamin Topical product for the prevention of eye irritation, and for prevention and therapy of blepharitis, comprises cobalamin in the form of cyano-, hydroxy- and/or methyl-cobalamin. - ACTIVITY : Ophthalmological; Antiinflammatory; Dermatological. - MECHANISM OF ACTION : None given.
CN101928279A 3-amino-2-pyrones cyclooxygenase inhibitors as well as preparation method and application thereof The invention relates to the field of medicinal chemistry, in particular to 3-amino-2-pyrones cyclooxygenase inhibitors (1) as well as a preparation method and the application thereof. R1 and R2 in a structural formula (1) are defined as the specifications. Proved by a pharmacological test, the 3-amino-2-pyrones cyclooxygenase inhibitors of the invention have the purposes as a cyclooxygenase selectivity inhibitor.
US6906090 Compositions and methods for treating mycobacterial diseases The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease.
CN102657640A PTP1B (protein tyrosine phosphatase 1B) inhibition activity of norathyriol, and application of norathyriol The invention which belongs to the technical field of biological pharmacy concretely relates to a PTP1B inhibition activity and an insulin resisting improvement of norathyriol, and an application of the norathyriol in PTP1B-correlated disease treating medicines. In-vitro enzyme inhibition experiments prove that the norathyriol is a competitive inhibitor of recombined human PEP1B, and the IC50 value is 9.2muM; and the norathyriol allows the sensitivity of normal C57BL/6 mice and ob/ob diabetes model mice to insulin to be obviously improved and the blood sugar of experiment animals to be reduced. So the norathyriol which is a novel PTP1B inhibitor can be used as a latent lead compound, and can be used for preparing medicines for treating metabolic syndromes of insulin resisting-correlated anti-diabetes, obesity and the like, tumors, and other PTP1B-correlated diseases.
EP1679064A2 Pharmaceutical compositions containing rapamycin derivatives A process for preparing an emulsion composition comprising an ascomycin or a derivative thereof as active agent, which process comprises the step of admixing to a placebo fat emulsion a concentrate comprising a) the active agent, b) a stabiliser selected from a phospholipid, a glycolipid, a sphingolipid, a diacylphosphatidyl glycerol, an egg-phosphatidylglycerol, a soy-phosphatidylglycerol, or a salt thereof; or a saturated, mono- or di-unsaturated (C12-24) fatty acid, or a salt thereof, and c) an organic solvent, wherein the weight ratio of acitve agent to stabiliser is between 400:1 and 0.5:1. The invention also provides ready-to-use emulsions, e.g. for intravenous administration, prepared using the above process.
WO2014008374A3 Combination therapies comprising metformin salts and antihyperglycemia agents or antihyperlipidemia agents The present invention is directed to a combination therapy comprising metformin eicosapentaenoate or metformin docosahexaenoate, or a mixture thereof, and an antihyperglycemic agent or an antihyperlipidemic agent, or a pharmaceutically-acceptable salt or prodrug thereof, or a pharmaceutically-acceptable salt of said prodrug. The invention further relates to methods of treating a metabolic disorder selected from the group consisting of type 2 diabetes (T2D), pre-diabetes, obesity, metabolic syndrome, hypertrilipidemia and T2D complications such as neuropathy, nephropathy, retinopathy, cataracts and cardiovascular complications, including cardiac arrhythmia, myocardial infarction, stroke, and cardiomyopathy in diabetic patients.
EP2643290A1 Calcium-sensing receptor-active compounds Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
CN1836664A Puerarin self-emulsifying microemulsified composition and its preparation method The self-emulsified puerarin micro emulsion composition contains puerarin, and micro emulsion system comprising polyoxyethylenefatty acid ester as the surfactant, medium carbon chain fatty acid ester as the oil phase and polyhydroxyl alcohol as co-surfactant. The preparation process includes dissolving puerarin in co-surfactan at 10-80 deg.c, cooling, mixing Tween-80 with surfactant, adding oil phase through stirring, and adding certain amount of water solution through stirring to form the micro smulsion. The self-emulsified puerarin micro emulsion composition has relatively high stability, and may be diluted with water into transparent low viscosity micro emulsion.
WO2007040006A1 Activator for peroxisome proliferator-activated receptor (pparϝ) and composition containing the activator for preventing or ameliorating specific symptom An activator for peroxisome proliferator-activated receptor Ϝ characterized by containing at least one compound selected from the group consisting of dehydroabietic acid, 13β-Δ8-dihydroabietic acid and isopimaric acid or a pharmaceutically acceptable salt thereof. This activator is useful in preventing or ameliorating at least one symptom selected form the group consisting of insulin resistance, type 2 diabetes, hyperlipemia, hypertension, obesity of the visceral fat type and fatty liver.
US20110117111 Microrna-based diagnostic testing and therapies for inflammatory bowel disease and related diseases The present invention is based, at least in part, on the novel discovery that certain microRNAs are associated with inflammatory bowel diseases and other related diseases. Accordingly, the invention relates to microRNA-based compositions, kits, and methods for detecting, characterizing, modulating, preventing, and treating inflammatory bowel diseases and other related diseases.
CN101148666B Nucleic acid adapter with high specificity and high affinity to human breast carcinoma tissue, preparation method and application thereof The present invention relates to one kind of nucleic acid gamete with high specificity and affinity to human breast cancer tissue and its preparation process and application. The nucleic acid gamete includes one DNA sequence and one RNA sequence and may be combined to human breast cancer tissue specifically, so that it may be applied for diagnosis and targeting treatment of human breast cancer. The nucleic acid gamete has high specificity and affinity to human breast cancer tissue and no reaction to health mammary gland tissue. The present invention also relates to derived sequences, including modified sequence, of the nucleic acid gamete.
CN101519410A Preparation method for metallic thiophene ring ternary complex with anti-cancer activity and application thereof The invention discloses a metallic thiophene ring ternary complex with anti-cancer activity. The complex has a chemical formula: RE(TTA)3L.nH2O(n=1-7) or Mt2(TTA)3L.Cl4. The complex has good chemical stability and thermal stability and can be used, stored and transported at a normal temperature. The ternary complex is 0.005 to 0.5 mu g/ml for the IC50 of a promyelocytic leukemia tumor cell, has a nanometer grade grain size range, and more easily enters and kills the cancer cell. In addition, the preparation method is simple, and has low preparation price, and little impact on the environment in a manufacturing link. The ternary complex has high biological availability and little dosage, and brings about less drug toxicity.
CN102370888A Anti-inflammation, skin ulcer converging and bleeding arresting medicament for treating gastritis, ulcer and bleeding and preparation method thereof The invention discloses an anti-inflammation, skin ulcer converging and bleeding arresting medicament for treating superficial gastritis, peptic ulcer and peptic bleeding and a preparation method thereof. The medicament is prepared into various medicaments by extracting active ingredients from rhubarb, garden burnet root, cuttlebone, common bletilla pseudobulb and liquoric root serving as raw materials with a water extraction method, decompressing with a single-effect process, concentrating at low temperature, refining, performing spray drying, grinding into powder serving as an active ingredient of the medicament, and combining the powder with a pharmaceutically acceptable excipient. The medicament has unique raw materials and preparation method, has the effects of resisting inflammation, diminishing swelling, regenerating tissue to heal ulcer, protecting the rennet, stopping gastric bleeding, and producing acid for reducing pepsin and eliminating rennet damaging factors, has a good adverse-rising energy calming function, and can be used for effectively treating superficial gastritis and peptic ulcer and quickly treating peptic bleeding. As proved by clinical experiments, the medicament has good curative effects on gastritis, ulcer and peptic bleeding, has no side effect, and has no toxic or side effect on human bodies and viscera.
US8362031 Lonidamine analogues and treatment of polycystic kidney disease Lonidamine derivatives can be useful in methods of treating, inhibiting, and/or preventing polycystic kidney disease (PKD). Accordingly, lonidamine derivatives can be administered in a therapeutically effective amount for inhibiting, and/or preventing polycystic kidney disease (PKD) in the subject. This can include administering a therapeutically effective amount of the lonidamine derivatives for inhibiting CFTR and/or Hsp90 or biological pathway thereof. Also, the method can include administering the lonidamine derivatives in a therapeutically effective amount for inhibiting ErbB2, Src, Raf-1, B-Raf, MEK, Cdk4, NKCC1, or combinations thereof. For example, the therapeutically effective amount of the lonidamine derivatives can be configured so as to provide a concentration in or adjacent to a kidney cell of about 0.25 uM or more or less.
CN102512365A Etimicin sulfate micelle freeze-dried powder injection and its preparation method The invention discloses an etimicin sulfate micelle freeze-dried powder injection and its preparation method. The powder injection comprises a therapeutically effective amount of etimicin sulfate, polyethylene glycol derived phospholipid, and pharmaceutically acceptable auxiliary materials. According to the preparation, the drugs are wrapped in a formed nano-micelle so as to be prepared into a nano-micelle preparation of etimicin sulfate for injection. The etimicin sulfate nano-micelle freeze-dried preparation in the invention not only reaches the long-acting circulation purpose in blood, and greatly enhances the bioavailability, but also substantially improves the stability of the preparation.
CN102040578A Method for preparing high purity tricin from bamboo leaves The invention discloses a method for preparing high purity tricin from bamboo leaves. The method comprises the following steps: (a) performing extraction on dry bamboo leaves with 95% ethanol, extracting with petroleum ether, concentrating aqueous phase to obtain extractum; (b) adding the extractum in an AB-8 macroporous resin column, eluting with pure water, then eluting with 80% ethanol, concentrating and drying eluent; (c) adding hydrochloric acid-methanol solution in the dry product obtained in the step (b), heating to perform acid hydrolysis process; (d) adding the acid hydrolysis solution obtained in the step (c) in a C18 column for elution chromatography, collecting tricin fraction, concentrating; and (e) adding the concentrate obtained in the step (d) in a gel separation column, using pure methanol as mobile phase to elute, collecting tricin fraction, and concentrating and drying to obtain tricin. In the invention, the simple method is used to obtain tricin with high yield and high purity.
CA2095708C Novel n-aralkyl- and n-heteroaralkyl-aminoalkanephosphinic acids N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids of formula I wherein R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical having at least 2 carbon atoms, R1 is hydrogen or hydroxy, R2 is an araliphatic or heteroarylaliphatic radical substituted by free or functionally modified carboxy that is bonded directly or by way of a spacer, and R3 is hydrogen, lower alkyl or a group R2, and the salts thereof have valuable nootropic and anti-epileptic properties and can be used in the preparation of a nootropic or anti-epileptic medicament.
EP2041068A1 Positively charged water-soluble prodrugs of ibuprofen with very fast skin penetration rate The novel positively charged pro-drugs of ibuprofen in the general formula (I) 'Structure 1' were designed and synthesized. The compounds of the general formula (I) 'Structure 1' indicated above can be prepared from functional derivatives of ibuprofen, (for example acid halides or mixed anhydrides), by reaction with suitable alcohols, thiols, or amines. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and pushes the pro-drug into the cytosol. The experiment results suggest that the pro-drug, diethylaminoethyl 2-(p-isobutylphenyl) propionate.AcOH, diffuses through human skin -250 times faster than ibuprofen itself and -125 times faster than ethyl 2-(p-isobutylphenyl) propionate. In plasma, more than 90% of these pro-drugs can change back to the drug in a few minutes. The prodrugs can be used medicinally in treating any ibuprofen-treatable conditions in humans or animals and be administered not only orally, but also transdermally for any kind of medical treatments and avoid most of the side effects of ibuprofen, most notably GI disturbances such as dyspepsia, gastroduodenal bleeding, gastric ulcerations, and gastritis. Controlled transdermal administration systems of the prodrug enables the ibuprofen to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of ibuprofen.
CN101283982A Fenofibrate nanometer suspension and preparation method thereof The invention belongs to the field of pharmaceutical preparations, and particularly relates to a fenofibrate nanosuspension and a lyophilized powder thereof. The fenofibrate nanosuspension is characterized in that poloxamer 188 and polyvinylpyrrolidone (PVP), with a weight ratio of (1-3):1, are used as surfactant. The fenofibrate nanosuspension has stable quality and particle diameter of about 190-380nm. The invention further discloses a preparation method thereof.
CA2809276A1 Food products comprising a slowly digestable or digestion resistant carbohydrate composition A food product comprises an oligosaccharide composition that is digestion resistant or slowly digestible. The oligosaccharide composition can be produced by a process that comprises producing an aqueous composition that comprises at least one oligosaccharide and at least one monosaccharide by saccharification of starch, membrane filtering the aqueous composition to form a monosaccharide-rich stream and an oligosaccharide-rich stream, and recovering the oligosaccharide-rich stream. Alternatively, the oligosaccharide composition can be produced by a process that comprises heating an aqueous feed composition that comprises at least one monosaccharide or linear saccharide oligomer, and that has a solids concentration of at least about 70% by weight, to a temperature of at least about 40°C, and contacting the feed composition with at least one catalyst that accelerates the rate of cleavage or formation of glucosyl bonds for a time sufficient to cause formation of non-linear saccharide oligomers, wherein a product composition is produced that contains a higher concentration of non-linear saccharide oligomers than linear saccharide oligomers.
US20050176788 Such as 2-[N-(4,5-dimethoxy-2-hydroxybenzoyl)amino]-4-[(2-diisopropylaminoethyl)aminocarbonyl]-1,3-thiazole; compounds relax gastric fundus, to relieve feeling of early satiety and bloating; gastrointestinal motility disorders A therapeutic agent for impaired gastric accommodation which contains as an active ingredient a compound represented by the general formula (1): (wherein R1 represents a hydrogen atom, a hydroxyl group or a halogen atom; A represents a furyl group, a thienyl group, a thiazolyl group or an oxazolyl group; R2 and R3 each represents an alkyl group with 1 to 5 carbon atoms; and n represents an integer of 2 to 4), or an acid addition salt thereof. Use of a therapeutic agent of the present invention greatly alleviates symptoms caused by said disorders, such as early satiety and bloating, because it improves relaxation of gastric fundus and impaired gastric accommodation.
US20080152654 COMPOSITIONS AND METHODS FOR siRNA INHIBITION OF ANGIOGENESIS Embodiments of methods of using siRNAs targeting VEGF including an siRNA defined by SEQ ID NO: 77 and SEQ ID NO: 78 to stabilize visual acuity in a subject, to inhibit choroidal neovascularization lesions, to treat age-related macular degeneration, to treat diabetic macular edema, and to decrease foveal thickness in subjects are disclosed. Additionally, methods of treating age-related macular degeneration and diabetic macular edema by administering combinatorial therapy comprising an siRNA targeting VEGF and a non-siRNA VEGF antagonist are described.
US20110217296 Method for selecting patients for treatment with an egfr inhibitor The present invention relates to cancer diagnostics and therapies and to the detection of alterations in cancer cells that are diagnostic, prognostic or predictive. In particular, the present invention provides a method for detecting and analyzing whether a patient suffering from a cancer is responsive to the treatment with an EGFR inhibitor. In the method, a tissue section from a cancer sample is subjected to assays based on immunohistochemistry and enzymatic metallography.
CN103316033A Gel and use thereof The invention belongs to the technical field of medicines, and discloses a gel and a use thereof. The gel comprises a chitosan polymer, a hyaluronic acid matter, a lactic acid matter, a gel matrix, a wetting agent and a diluter. The gel has the advantages of good antibacterial effect, wide antibacterial spectrum (comprising high risk HPV (Human Papilloma Virus), physical antibacterial effect, no tolerance, biodegradability, safety and environment-friendliness and lasting effect for a long time, and has the functions of nourishing, lubricating, whitening, repairing skins or mucosal tissues, and removing spots and inhibiting cicatrisation for skins or mucosal tissues.
US20070099855 Glycyrrhizin or derivatives thereof for for treating or preventing severe acute respiratory syndrome (sars) The invention provides methods for preventing, treating, managing or ameliorating viral infections, in particular, Severe Acute Respiratory Syndrome (SARS). More specifically, the invention provides methods for preventing, treating, managing or ameliorating a SARS-associated coronavirus or one or more symptoms thereof by administering Glycyrrhizin and/or derivatives thereof The invention also provides methods for preventing, treating, managing or ameliorating a SARS-associated coronavirus or one or more symptoms thereof by administering Glycyrrhizin and/or a derivative thereof in combination with a prophylactic or therapeutic agent other than Glycyrrhizin or a derivative thereof.
WO2005106471A3 Diagnostics and therapeutics for diseases associated with c-c chemokine receptor 4 (ccr4) The invention provides a human CCR4 which is associated with the cardiovascular disorders, gastrointestinal and liver diseases, inflammatory diseases, metabolic diseases, hematological disorders, cancer disorders, neurological disorders, respiratory diseases and reproduction disorders. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular disorders, gastrointestinal and liver diseases, inflammatory diseases, metabolic diseases, hematological disorders, cancer disorders, neurological disorders, respiratory diseases and reproduction disorders. The invention also features compounds which bind to and/or activate or inhibit the activity of CCR4 as well as pharmaceutical compositions comprising such compounds.
US20090281068 Polylactide compositions and uses thereof The present invention provides compositions and methods relating to polylactides which may be used for drug delivery (e.g., parenteral delivery), wherein an organic solvent is not required.
US20070265331 Such as (2S)-2-(3(S)-Acetylamino-3-((S)-sec-butyl)-2-oxo-pyrrolidin-1-yl)-N-[(1S,2R)-1-(3,5-difluoro-benzyl)-2-hydroxy-3-(3-methoxy-benzylamino)-propyl]-4-phenyl-butyramide; inhibit processing of amyloid precursor proteins There is provided a series of novel substituted gamma-lactams of Formula (I) wherein R1, R2, R3, R4 and R5 are defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present invention is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
US20100278772 Dna methylation markers and methods of use The present invention provides methods for identifying metastases by detecting nucleic acid hypermethylation of one or more genes in one or more samples, and in particular in the lymph nodes. The invention further relates to DNA methylation as a predictor of disease recurrence and patient prognosis, specifically in the field of cancer biology.
US20110201645 Method Of Treating Attention Deficit Disorders With D-Threo Methylphenidate Methods for treating Attention Deficit Disorder, Attention Deficit Hyperactivity Disorder, AIDS Dementia Complex and cognitive decline in HIV-AIDS while minimizing drug hypersensitivity, toxicity, side effects, euphoric effect, and drug abuse potential by administration of d-threo-methylphenidate or pharmaceutically acceptable salts thereof.
WO2004089396A3 Anti-fungal peptidomimetics The invention relates to compounds including peptides and peptidomimetics having anti-fungal activity alone, and in combination with other agents that have anti-fungal activity. The invention includes the use of cell cycle G2 checkpoint abrogators as anti-fungal agents, such as anti-fungal medicine.
WO2012122106A2 Compositions and methods apc, creb, and bad pathways to assess and affect cancer Disclosed are compositions and methods for assessing the apoptosis and survival BAD phosphorylation pathway (BAD pathway); and/or (2) the cell cycle role of APC in cell cycle regulation pathway (APC pathway); and/or (3) the transcription CREB pathway (CREB pathway) and for using these pathways to assess, treat, monitor, prognose, diagnose, etc. subjects with cancer. Also disclosed are compositions and methods for identifying molecular pathways that are common to one or more chemotherapeutic agents for the treatment of an oncological disorder, for screening for compounds or agents that can be used to treat ovarian cancer, and for selecting for compounds or agents that can enhance the cytotoxic response of cisplatin, carboplatin, and/or paclitaxel against a cancer cell, such as an ovarian cancer cell or cell line. In some forms, the disclosed methods can comprise identifying compounds and/or agents that modulate the BAD pathway and/or the APC pathway; and/or the CREB pathway. In some forms, the disclosed methods can comprise method for treating cancer using compounds and/or agents that modulate the BAD pathway and/or the APC pathway; and/or the CREB pathway. Also disclosed are compositions, compounds, and agents identified using the disclosed methods.
WO2013124169A1 Use of 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors 1 H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors. The present invention relates to the 1 H-indazole-3-carboxamide compounds for use as glycogen synthase kinase 3 beta (GSK-33) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies.
US20120135091 Methods and compositions for enhancing lifespan involving sirtuin-modulating compounds and chalcogenides The present invention concerns the use of active compounds, including chalcogenides and sirtuin-modulating compounds, either alone or in combination for increasing or enhancing survivability and/or longevity in biological matter. In general aspects, the chalcogenides and other active compounds may modulate one or more sirtuin proteins. It includes compositions, methods, articles of manufacture and apparatuses for enhancing survivability in any of these biological materials, so as to preserve and/or protect them. In specific embodiments, there are also therapeutic methods and apparatuses for aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, organ transplantation, hyperthermia, wound healing, hemorrhagic shock, cardioplegia for bypass surgery, neurodegeneration, hypothermia, and cancer using the active compounds described.
US20050250832 For increasing blood-brain barrier permeability The present invention provides novel benzimidazol-2-one derivatives useful as therapeutic agents.
WO2012038438A1 4,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) The present invention relates to novel 4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-yl- aminederivativesas inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretaseis involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associatedwith stroke, dementia associated with Parkinson's disease or dementia associated with beta- amyloid.
CN1565459A Dermatopathy therapeutic medicine compositions and its preparation method The invention relates to a dermatopathy therapeutic medicine compositions and its preparation method, in particular a propylene amine antimycotics, and suprarenal hormones medicinal compositions and its preparation method.
CA2177772C Pharmaceutical compositions containing irbesartan Pharmaceutical compositions containing irbesartan, alone or in combination with a diuretic, providing tablets with a high relative amount of active agent and excellent wetting and disintegration properties.
CN102552228A Application of vitamin K to preparation of pyruvate kinase inhibitor The invention provides two inhibitors of M2 type pyruvate kinase (PKM2)-vitamin K type compounds (vitamin K3 and vitamin K5). The currently reported PKM2 inhibitor which belongs to small molecular compounds is Compound 3 only. The effect of the vitamin K on inhabitation of the PKM2 is found to be higher than that of the Compound 3. Therefore, as an inhibitor of pyruvic acid, the vitamin K has important application value. Two new pyruvate kinase inhibitors-vitamin K3 and vitamin K5 are provided, provide basis for selection of new medicaments and have important application prospect.
WO2011124697A1 Antimicrobial compounds of 1,4- naphtoquinone structure The present invention relates to a compound having formula (I) wherein: R1 is chosen from the group consisting of: phenyl group, possibly substituted, -CH2-C6H4-R'1 group, R'1 being chosen from the group consisting of: H, -OH, halogen, alkyl, aryl, CHO, -CN, -NO2, -SRα, -ORα, - NRαRβ, -CONRαRβ, -COORα, and -NHCORα, Rα and Rβ representing independently from each other H, an alkyl group or an aryl group, R'1 being preferably in para position, and -CH2-CO-R' group, R' representing an aryl or heteroaryl group, said aryl and heteroaryl groups being possibly substituted, R2 is chosen from the group consisting of: -OH and halogen, and R3, R4, R5 and R6 are in particular H, for its use for the prevention and/or the treatment of bacterial infections.
WO2013109142A1 Combined pdk and mapk/erk pathway inhibition in neoplasia The current inventors have found a new method for treatment of malignant neoplasia. In particular the invention relates to the field of treating neoplasia in subject in need thereof and that involve (activated) MAPK/ERK pathway proteins, like BRAF melanomas and the like. Compositions for use in such treatment are provided which make use of pyruvate dehydrogenase kinase (PDK) inhibitors.
CN101411714A Chemical substance for treating colpitis The invention provides a chemical substance for treating colpitis and belongs to the field of medical appliance and medicine. The chemical substance is characterized by being oligoisomaltose or containing the oligoisomaltose; the composition containing the oligoisomaltose comprises oligoisomaltose and a carrier, wherein the weight percentage of the oligoisomaltose is between 1 and 99 percent, and the weight percentage of the carrier is between 1 and 99 percent. Compared with the prior art, the chemical substance adopted by the invention can obviously promote growth of lactic acid bacillus owned by the colpitis, and obviously suppress growth of staphylococcus aureus, colon bacillus and candida albicans, thereby restoring flora balance for the colpitis, and playing roles of preventing and treating colpitis mycotica and bacterial vaginitis.
WO2014006091A1 Ticagrelor adducts with divalent metal salts The present invention relates to amorphous adducts of ticagrelor with divalent metal salts useful in the treatment or prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease.
CN1923207A Compound recipe vitamin freeze-dried powder for injection and its preparing process The invention relates to a composite vitamin freeze dried and relative production. Wherein, said method comprises (1), adding alcohol dissolved with antihypertensive, with vitamin A palmitate, vitamin D2, vitamin E acetic ester and vitamin K1, and adding 10% injection water, adding stabilizer and dissolving; (2), dissolving support agent into 70% injection water, adding 0.01-0.1% active carbon, mixing for 5-30mins, filtering, and collecting acetic ester; (3), mixing the products of steps (1, 2), adding injection water to full, using pH adjuster to adjust the pH valve to 7.4-7.6, using 0.2-0.4 mum porous membrane to filter, and freezing. The invention has fine frozen crystal, quick dissolution, and highs stability.
CA2544963C Myo-inositol hexaphosphate for topical use technical field The invention relates to a composition that includes myo-inositol hexaphosphate in a form adapted to topical administration for utilisation in the treatment or prevention of a disease associated with the development of heterogeneous nucleants in a soft tissue. Said composition can be used for manufacturing a drug for the treatment of a disease associated with the development of heterogeneous nucleants in a soft tissue.
EP1771442A1 Viral polymerase inhibitors A compound, represented by formula (I) or an enantiomer, diastereoisomer or tautomer thereof : wherein either A or B is nitrogen and the other B or A is C, and the radicals R1, R2, R3, R5, R6, R7, R9, and R10 are as defined herein, or a salt, ester or derivative thereof as viral polymerase inhibitors. The compound is used as an inhibitor of RNA dependent RNA polymerases, particulary those viral polymerases within the Flaviviridae family, more particulary to HCV polymerase.
US20090028930 Bruise amelioration composition and method of use A bruise amelioration composition that can be applied for one hour to an affected site, such as a bruise, contusion or blister, in the form of a gel, liquid or adhesive bandage. The composition includes at least 40% by weight of glycerin and at least 2% by weight of primrose oil. Preferably, the composition includes a fragrance, such as peach oil and marjoram and 1% to 10% by weight of vitamins A, C, D, E and K.
US20080050446 Fast Release Dosage Forms for Antibiotics A multiparticulate, pharmaceutical dosage form containing at least one antibiotic which is sparingly wettable with aqueous media or sparingly soluble in aqueous media and a combination of carrageenan and tricalcium phosphate and optionally sucrose ester. Also, an administration system having this dosage form arranged in a drinking straw with at least one barrier device for single administration, optionally together with a conveying liquid.
CN101880286A Water-soluble amino-acid ester derivative of ginkgolide B The invention relates to an amino-acid ester derivative of ginkgolide B shown as a formula I and pharmaceutical salts thereof, a medicinal composition taking the compounds as active ingredients, and application of the compounds and the medicinal composition in serving as medicaments for treating cardiovascular and cerebrovascular diseases. In the formula I, A1 and A2 is residues of H, glycyl, L-alanyl, L-leucyl, L-valyl, L-isoleucyl, or L-phenylaminoacyl and other amino acids; A1 is the same as or different from A2; and A1 and A2 cannot be H at the same time.
CN103694258A Spiro-condensed 1, 3, 4-thiadiazole derivatives for inhibiting ksp kinesin activity The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity. Formula I [Chemical formula should be inserted here as it appears on abstract in paper form.
DE102004063269A1 New 9,10-dihydroxy-1,4-dihydroanthracene-1,4-dione compound is protein kinase D inhibitor useful for tumor suppression, inhibition of tumor angiogenesis and the treatment of cancers 9,10-Dihydroxy-1,4-dihydroanthracene-1,4-dione compound (I), as an agent for tumor suppression and inhibition of tumor angiogenesis, is new. 9,10-Dihydroxy-1,4-dihydroanthracene-1,4-dione compound of formula (I), as an agent for tumor suppression and inhibition of tumor angiogenesis, is new. Independent claims are also included for: (1) a pharmaceutical composition (A) comprising (I), carriers and diluents; and (2) a method for preparing (A) comprising mixing (I) with one or more carriers and diluents and bringing the mixture into a suitable administration form. [Image] - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : Tumor angiogenesis inhibitor; Protein kinase 2 inhibitor; Protein kinase D inhibitor. The protein kinase D inhibitory activity of (I) was tested using HeLa cells in a biological assay. The results showed that the median inhibitory concentration of (I) is 39.69 mu M.
WO2009140215A3 Method for treating drug-resistant bacterial and other infections with clioquinol, phanquinone, and related compounds The invention relates to new uses of known chelating compounds for the treatment of bacterial in fungal infections, particularly by methicilllin-resistant and other drug-resistant strains of bacteria and fungi. One of more chelating compound is administered with or without additional antibiotic or antifungal drugs to achieve improved therapy. Preferred chelating compounds include clioquinol, 5,7-dichloro-8-hydroxy-quinaldine, phanquinone, 5,7-dichloro-8-hydroxyquinoline, 5,7- di-iodo-8-hydroxyquinoline. By chelation of specific metal ions, these compounds treat any infection by bacteria or fungi whose pathogenicity depends upon metalloenzymes that require these cations. The compounds are also effective against infections caused by extended β lactamase and metallo β lactamase producing bacterial strains. Bacteria targeted by these methods include methicillin-resistant Staphylococcus aureus, penicillin resistant or intermediate resistant Streptococcus pneumoniae and other gram positive and multiresistant gram negative species and strains.
US20080050444 Pharmaceutical compositions of ilaparazole The present invention relates to pharmaceutical compositions comprising solid particles of an active ingredient that have a particle size of from about 0.1 micron to about 100 microns.
WO2014005597A1 Rose hip composition, process for the manufacture of the rose hip composition and said composition for use in a method for the maintenance of flexible joints and decreased inflammation The present invention relates to a composition comprising dried rose hip powder and added vitamin C, wherein the dried rose hip is obtainable by a process comprising the steps of providing harvested rose hip, drying and chopping the rose hip, separating the chopped rose hip and isolating the shells, grinding the shells, and optionally sieving the ground rose hip shells, wherein the grinding is performed at a substantially constant temperature, said temperature being below ambient temperature, such as 40°C.
US20080188430 RNA interference mediated inhibition of hypoxia inducible factor 1 (HIF1) gene expression using short interfering nucleic acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating hyproxia inducable factor (e.g., HIF1) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of HIF1 gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of HIF1 genes.
US20080241251 Method of Producing Microparticles A method of producing microparticles having a median diameter up to 100 μm and the microparticles so produced are described. The method includes the steps of providing a solvent having a bioactive dispersed or dissolved therein and a vehicle dissolved therein, carrying out an emulsification in a non-solvent phase to produce an emulsion containing the bioactive and the vehicle in a solvent phase, and evaporating the solvent to leave the microparticles, wherein a mixture of at least two surfactants is employed to stabilize the emulsion and wherein the mixture has a hydrophilic-lipophilic balance (HLB) of up to 8.
US7803811 1-methoxy-2-methyl-3-[(4-nitrophenyl)sulphonyl]indolizine, used as angiogenesis inhibitors The present invention relates to novel 1,2,3-substituted indolizine derivative which are inhibitors of fibroblast growth factors, to methods or preparing such derivatives, to pharmaceutical compositions comprising such derivatives, and to methods of treatment comprising such derivatives.
EP2332543A1 Tetrahydrobenzazepines and their use in the modulation of the dopamine D3 receptor The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to a compound according to the present invention for use in treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.
US7879849 such as 1-(2-Methylpropyl)-2-propyl-2H-pyrazolo[3,4-c]quinolin-4-amine, used as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of viral and neoplastic diseases Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, and 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
WO2013179067A1 An icam-1 anti sense for the treatment of inflammation and pain in a rectal stump This invention relates to a composition comprising an antisense oligonucleotide that down- regulates intracellular adhesion molecule-1(ICAM-1) for use in treating inflammation, pain and/or discharge in a rectal stump.
CN102940629A New use of Tubacin The invention discloses a new use of Tubacin and provides an application of the Tubacin to production preparation. The use of the Tubacin is at least one of the following uses of (1)-(5): (1) restraining microtubule destruction; (2) increasing microtubule acetylization levels; (3) restraining neuro muscule junction (NMJ) paramorphia; (4) restraining NMJ microtubule skeleton anomalies; and (5) treating alzheimer's diseases. The Tubacin has a far-reaching significance for analyzing pathogenesis of the alzheimer's diseases and has a significant value in researching and developing drugs of the alzheimer's diseases and treating the alzheimer's diseases.
US7166708 Reacting a protein with a hapten (especially a luteinizing hormone releasing hormone peptides derived from E coil, or malaria derived peptides) to produce a hapten-protein conjugate, followed by reacting the hapten-protein conjugate with a polysaccharide This invention relates to a process for preparing a hapten-protein-polysaccharide conjugate and a hapten-protein conjugate by reacting a protein with a hapten to produce a hapten-protein conjugate, followed by reacting the hapten-protein conjugate with a polysaccharide to provide a conjugate mixture including the hapten-protein conjugate and a hapten-protein-polysaccharide conjugate. This invention also includes the process described above with the addition of a pharmaceutically acceptable medium or delivery vehicle into the conjugate mixture. The invention further includes the process described above where the hapten is luteinizing hormone releasing hormone peptides derived from E coil, or malaria derived peptides.
CN102309467A Preparation method of atorvastatin calcium capsule The invention provides a preparation method of an atorvastatin calcium capsule preparation, and the method comprises the following steps: uniformly mixing amorphous atorvastatin calcium with a water-soluble solid dispersion carrier; heating to melt the solid dispersion carrier, and cooling and curing after the amorphous atorvastatin calcium is uniformly dispersed in the molten dispersion carrier; drying the obtained mixture at a low temperature to obtain mixture particles; and then mixing the obtained particles with other medicinal auxiliary materials, and filling into capsules. By utilizing the preparation method provided by the invention, the dispersion degree of the atorvastatin calcium raw material is improved, the granularity of the medicament is reduced, and the specific surface area is increased, so that the dissolution rate is improved.
DE102007045241A1 Cosmetic preparation, useful as an agent that is effective against e.g. gram negative and gram positive bacteria, yeast and/or fungus, comprises piroctone olamine and stabilizing agent e.g. benzaldehyde and/or alkane-diol Cosmetic or dermatological preparation (I) comprising one or more piroctone olamine and one or more stabilizing agent including benzaldehyde and/or alkane-diol and/or -triol. - ACTIVITY : Antibacterial; Fungicide. - MECHANISM OF ACTION : None given.
CN101503440A Nucleic acid molecule SI-CYPJ-12 and use thereof in anti-cancer medicine preparation The invention belongs to the biological medicine field, relating to nucleotide molecules and the application thereof in the preparation of antitumor medicines. The invention provides the nucleotide molecules for preparing the antitumor medicines. The nucleotide molecules have the activity for inhibiting the tumor growth and the sequence thereof comprises 5'-GUGUUGCCUCCUCUUCCAG-3'or 5'-GTGTTGCCTCCTCTTCCAG-3' which is known as SI-CYPJ-12 in the invention. The nucleotide molecules SI-CYPJ-12 can obviously inhibit the tumor cell proliferation; when the nucleotide molecules are applied to a naked mouse, the tumor body growth of the naked mouse is obviously inhibited compared with the control naked mouse in the same condition of culture, and the phenomenon becomes obvious day by day as time goes on. The invention provides a new approach and means for the tumor treatment and mitigation.
US20060135444 Combination of flavonoid and procyanidin for the reduction of the mammalian appetite A nutritional composition suitable for reducing appetite, a method for the treatment and/or prevention of overweight and a method for the reduction of a mammalian appetite. The weight reduction and/or appetite reduction is achieved by administration of procyanidin and a flavonoid selected from the group consisting of chrysin, flavone, precursors of these flavonoids that are convertible into the one of these flavonoids by gastrointestinal hydrolytic cleavage and mixtures thereof.
CN102379845A Aprepitant microemulsion for injection and preparation method thereof The invention discloses an aprepitant microemulsion for injection. The aprepitant microemulsion consists of the following components in percentage by mass: 0.05 to 2 percent of aprepitant, 5 to 30 percent of oil for injection, 0.5 to 10 percent of emulsifier, 1 to 10 percent of co-emulsifier, 5 to 20 percent of protective agent and 60 to 80 percent of water for injection. Compared with the conventional oral aprepitant, the aprepitant microemulsion for the injection has the outstanding advantage that: the aprepitant is insoluble in the water and an organic solvent, in order to realize the aprepitant injection, the aprepitant microemulsion and aprepitant micro emulsion freeze-drying powder are prepared successfully and can be subjected to large-scale industrial production; and compared with a fosaprepitant dimethyl-meglumine injection, the aprepitant microemulsion has the advantages that: the cost is reduced greatly, the practicality is extremely high, and economic and social benefits are relatively good.
US20050176740 Synergistic for cancer characterized by ras oncogene overexpression; N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering an erb family inhibitor and a Raf and/or ras inhibitor to a mammal suffering from a cancer.
CN103127133A Inhalation drug composition with fluticasone propionate and nitric oxide synthase (NOS) inhibitor An inhalation drug composition with fluticasone propionate and a nitric oxide synthase (NOS) inhibitor comprises the fluticasone propionate which serves as an active ingredient, an amino acid derivative which serves as the NOS inhibitor and one or more drug auxiliary materials which suit to be inhaled.
CA2399377C New positive allosteric ampa receptor modulators (paarm), processes for preparing them and their use as pharmaceutical compositions The present invention relates to new positive allosteric AMPA receptor modulators of general formula (I) (see formula I) wherein R1, R2 R3, R4, R5 and R6 may have the meanings indicated in the specification and claims, processes for preparing them and their use as pharmaceutical compositions.
CA2238277C Compositions and therapeutic methods using morphogenic proteins and stimulatory factors The present invention provides pharmaceutical compositions comprising a morphogenic protein stimulatory factor (MPSF) for improving the tissue inductive activity of morphogenic proteins, particularly those belonging to the 13MP protein family. Methods for improving the tissue inductive activity of a morphogenic protein in a mammal using those compositions are provided. This invention also provides implantable morphogenic devices comprising a morphogenic protein and a MPSF disposed within a carrier that are capable of inducing tissue formation in allogeneic and xenogeneic implants. Methods for inducing local tissue formation from a progenitor cell in a mammal using those devices are also provided. A method for accelerating allograft repair in a mammal using morphogenic devices is provided. This invention also provides a prosthetic device comprising a prosthesis coated with a morphogenic protein and a MPSF, and a method for promoting in vivo integration of an implantable prosthetic device to enhance the bond strength between the prosthesis and the existing target tissue at the joining site. Methods of treating tissue degenerative conditions in a mammal using the pharmaceutical compositions are also provided.
CN103550200A Application of pharmaceutical composition in preparation of medicament for inhibiting blood sugar rise and medicament for reducing blood fat The invention provides a preparation method of a ketone pharmaceutical composition extracted from hypericum japonicum. The pharmaceutical composition obtained by using the method mainly contains 6-deoxidized isojacareubin, isojacareubin, hypericum japonicum diketone, 1,3,5,6-tetrahydroxy-4-isoamyl alkenyl ketone, hypericum japonicum diketone C and the like. A pharmacodynamic experiment result shows that the composition has the effects of inhibiting blood sugar rise and reducing blood fat, and can be applied to preparation of a medicament for preventing and treating diabetic syndrome and hyperlipidemia caused by high blood sugar.
CN101837116A Liver-protecting and alcoholism-relieving product using Saccharomyces cerevisiae as main material The invention provides a liver-protecting and alcoholism-relieving product using Saccharomyces cerevisiae, which contains over 42 percent of proteins, more than 500 milligrams of total B vitamins per kilogram and more than 800 milligrams of glutathione per kilo gram, as main materials. The invention also provides a method for producing the liver-protecting and alcoholism-relieving product.
EP2633886A1 Compounds and mixtures influencing inflammatory states Suggested is a compound of the formula (X) or any salt of a compound of the formula (X) or any mixture containing or consisting of two or more different compounds of the formula (X), two or more different salts of compounds of the formula (X) or one or more different compounds of the formula (X) and one or more different salts of compounds of the formula (X), wherein for R1, R2 and R3 independently of one another in every compound of the formula (X) the following applies: R1 means hydrogen or methyl, R2 means an organic residue with 5 carbon atoms and one oxygen atom or none and R3 means an organic residue with 10 carbon atoms and one or more oxygen atoms, or R1 and R2 together with the carbon atoms in positions 4 and 5 and the oxygen atom bound to the carbon atom in position 4 form a ring and comprise 5 carbon atoms and one oxygen atom or none, and R3 means an organic residue with 10 carbon atoms and one or more oxygen atoms, for use in a method for the prophylaxis and/or treatment of inflammation.
US20090162440 Sodium alginate microsphere vascular embolus containing water-soluble drug and preparation and application thereof The present disclosure relates to a kind of sodium alginate microsphere vascular embolus that contains water-soluble drug and preparation and application thereof. The embolus preparation falls into dry microsphere type and wet one that are made of degradable materials. The drug carrier can be sodium alginate, human serum albumin, chitosan or sodium hyalurate, solidifying and forming microsphere together with calcium ion solution under presence of static charge. The microsphere can have a diameter in the range of 20-1000 μm and can be divided into a wide variety of sizes in case of need. The present disclosure adopts raw materials that are good at mechanical strength, bio-compatibility, bio-degradability and stability. In vitro experiments, animal trials and clinical observations reveal that this embolus is a good targeting medication for embolism treatment and immunochemotherapy, which is safe, effective for the treatment of solid tumors including primary liver cancer, lung cancer, renal tumors, bladder cancer, uterine cancer, ovary cancer, colon carcinoma and rectal cancer.
CN101972419A Medicinal composition for preventing sunstroke and reducing temperature of milk cow and preparation method thereof The invention relates to a medicinal composition for preventing sunstroke and reducing temperature of a milk cow and a preparation method thereof. The medicinal composition is characterized by mainly comprising the following medicaments in part by weight: 11 to 15 parts of root of rehmannia, 8 to 12 parts of airpotato yam rhizome, 8 to 12 parts of talc, 14 to 18 parts of reed rhizome, 31 to 35 parts of green bean and 14 to 18 parts of bamboo leaf. The preparation method comprises the following steps of: weighing the six medicaments as raw materials according to the weight ratio; adding water in an amount which is 4 times the amount of the medicaments; decocting the medicaments twice, 1.5 hours every time; combining the decoction; filtering; standing the filtrate for 12 hours; concentrating supernatant; adding ethanol until alcohol content is 60 percent; and placing, filtering, adding water, filtering, filling and sealing and circulating steam at the temperature of 100 DEG C for 30 minutes. The medicinal composition and the preparation method have the following advantages that: the components in the composition are together used for preventing sunstroke and reducing temperature; the situation that the method for preventing sunstroke and reducing temperature in cow raising industry is simple and medicaments are in short supply is changed; and the composition has the characteristics of high safety factor, quick response, definite therapeutic effect, no medicament residue and no toxic or side effect.
US7132416 Benzothiazepine and benzothiazepine derivatives with ileal bile acid transport (IBAT) inhibotory activity for the treatment hyperlipidaemia The present invention relates to compounds of formula (I) wherein Rv, R1, R2, Rx, Ry, M, Rz, v, R3, R4, R5 and R6 are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.
CN103393656A Application of Sarcaboside A to medicament for resisting lung cancer metastasis The invention discloses application of Sarcaboside A to preparation of medicaments for resisting lung cancer metastasis and belongs to the technical field of novel application of medicaments. The Sarcaboside A can inhibit motion and migration capability of tumor cells. The application of Sarcaboside A to the preparation of medicaments for resisting lung cancer metastasis involved in the invention is disclosed for the first time. The Sarcaboside A has a novel skeleton type and unimaginably strong activity in inhibition of lung cancer metastasis.
US20120094965 Method and Formulation for Chemical Peeling A chemical peeling formulation and a formulation able to increase the efficacy and the tolerability of preparations based on the use of compounds used to carry out chemical peeling, comprising at least one keratolytic agent and dimethyl isosorbide. The composition may additionally comprise dimethyl sulphone.
US20110033557 Pharmaceutical composition and diagnostic and therapeutic use thereof A pharmaceutical composition comprises a diluted water solution containing hydrogen peroxide between about 1% and about 40%, at least a stabilizing compound comprised between about 0% and about 0.2% and at least synergizing compound comprised between about 0% and about 1.5% in weight.
CN103739651A Preparation method of panax japonicus Ib and application of panax japonicus Ib in preparation of inhibitory drug fibrinolytic enzyme original activator inhibitor (PAI-1) The invention discloses a preparation method of panax japonicus Ib. The preparation method comprising the following main preparation steps: by taking panax japonicus as a raw material, breaking, carrying out aqueous extraction by using 70% ethanol, and concentrating an extracting solution; extracting n-butanol, merging the extracting solution of an extraction layer, concentrating into 0.05-0.1g/ml concentrate, adding acetone into the concentrate as a precipitator, fully precipitating, and drying under reduced pressure to obtain crude extract; taking the crude extract, enriching through an MCI conical adsorption chromatography, removing impurity by using a 30% ethanol-water mixture, eluting by using a 60-80% ethanol-water mixture, collecting eluent, and drying to obtain total saponins; and separating the total saponins by a conical silica gel chromatography, collecting corresponding fractions, recovering a solvent under reduced pressure, and drying to obtain the panax japonicus Ib. The panax japonicus Ib has PAI-1 inhibitory activity, and can be used in the clinical treatment of diseases caused by fibrinopeptide disorders, such as deep venous thrombosis, coronary heart disease and pulmonary fibrosis.
US6894047 Triazine compounds useful as sorbitol dehydrogenase inhibitors This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula I wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing these compounds and to methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy, diabetic cardiomyopathy and foot ulcers. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of the present invention with a second pharmaceutical agent, including an aldose reductase inhibitor, a sodium hydrogen ion exchange inhibitor, a glycogen phosphorylase inhibitor, a selective serotonin reuptake inhibitor, a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, an angiotensin converting enzyme inhibitor, a thiazolidinedione antidiabetic agent, an angiotensin II receptor antagonist, a γ-aminobutyric acid agonist, a phosphodiesterase type 5 inhibitor, an adenosine agonist, and a CETP inhibitor and to methods of using these compositions.
US7166582 Administering stachyose to treat atopic dermatitis; can be added to medicine, food and beverage The present invention provides a sate and excellent antiallergic composition, and more particularly a preventive and therapeutic composition for atopic dermatitis, including an antiallergic composition blended with stachyose as an effective ingredient, and a medicine, food and beverage containing the composition.
WO2014015760A1 Crystal form of cabazitaxel and preparation method thereof The present invention relates to the field of medical chemistry, and discloses a preparation method for three crystal forms of cabazitaxel, that is, ester compound crystalline form J of cabazitaxel, hydrate crystalline form G of cabazitaxel and crystalline form I of cabazitaxel, and a novel crystalline form of cabazitaxel. The novel crystalline form of cabazitaxel according to the invention has good stability and good solubility in commonly used solvents, and is easy to be preserved and is stable under treatment during preparation of dosage forms,thus could be used for the preparation of drugs for treating prostate cancer.
WO2009049422A1 Compositions and methods for enhancing enzyme activity in gaucher, gm1 -gangliosidosis/morquio b disease. and parkinson's disease Therapeutic compositions and methods for treatment of lysosomal storage disorders, such as Gaucher, GM1-gangliosidosis/Morquio B disease and Parkinson's disease are described herein. The compositions comprise compounds having glucocerebrosidase and beta-galactosidase inhibitory activity for use as pharmacological chaperones for mutant forms of the enzyme. Methods of treatment involve providing therapeutically effective amounts of 5[(4-methylphenyl) thio] quinazoline-2,4-diamine) to subjects in need thereof.
US20100159021 Small Molecule Ligands of the Integrin RGD Recognition Site and Methods of Use Provided herein are compositions and methods for treating cancer by increasing the pro-apototic actions of small molecule ligands of integrin RGD recognition sites such as polyphenols by administering such compounds in conjunction with anti-angiogenic thyroid hormone analogs such as tetrac or triac.
US20080275027 Piperazinone Derivatives Useful as Histamine H3 Receptor Antagonists and/or Inverse Agonists The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis: wherein R1 and R2 are as defined in the specification.
EP1177796B1 Medicament for prevention or therapeutic treatment of liver disease Preventives/remedies for liver diseases which contain compounds having an Rho kinase inhibitory activity; and liver astrocyte activation inhibitors. Because of having excellent effects of inhibiting the activation of liver astrocytes, preventing the fibrosis of liver tissues, etc., compounds having an Rho kinase inhibitory activity (for example, (+)- trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl) cyclohexane) are useful in preventing and treating various liver diseases such as hepatitis, hepatic fibrosis, liver cirrhosis and liver cancer.
CN1990485A Silybin flavonolignan and their production method and use The invention relates to a silibinin flavonolignan and its medicine salt or solvates. The invention also relates to the method preparing its important mediate and its drug combination and medical application. The compound can protect primary hepatocyte from oxidative damage for SD newly born rat hepatitis virus, so it is expected to be used as drug preventing liver damage. The compound can remove superoxide anion free radical and diphenyl picryl phenylhydrazine free radical, inhibit free radical from inducing generation of fat oxidatant, protect PC 12 cell from being damaged by free radical, so it is expected to be used as drug treating diseases caused by free radical.
WO2006057886A3 2-METHYLENE-19,26,27-TRINOR-(20S)-1α-HYDROXYVITAMIN D3 AND ITS USES This invention discloses 2-methylene-19,26,27-trinor-(20S)-vitamin D analogs, and specifically 2-methylene-19,26,27-trinor-(20S)-lα-hydroxyvitamirt D3 and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
US7629003 Esters of L-carnitine of alkanoyl L-carnitines useful as cationic lipids for the intracellular delivery of pharmacologically active compounds Esters of L-carnitine and alkanoyl L-carnitines are described which can be used as cationic lipids for the intracellular delivery of pharmacologically active compounds. New esters of L-carnitine and alkanoyl L-carnitines of formula (I) are also disclosed wherein the R groups are as defined in the description.
WO2009093141A3 Novel inhibitors of mycobacterium complex cytochrome p450 cyp121 The present invention relates to the identification of the cyclodipeptide cyclo(L-Tyr-L-Tyr) as substrate of CYP121 from Mycobacterium tuberculosis, to the crystal structures of CYP 121 complexed either with cyclo(L-Tyr- L-Tyr) or with other cyclodipeptides, to the use of these structures in rational drug design methods to generate cyclodipeptide-based molecules that could inhibit CYP 121 activity, and to the design of new anti-Mycobacterium tuberculosis agents based on the DKP scaffold.
US20060004026 Compositions for ameliorating attention-deficient/hyperactivity disorder A composition for ameliorating attention-deficit hyperactivity disorder, characterized in that the composition comprises theanine; and a method of ameliorating attention-deficit hyperactivity disorder comprising the step of administering theanine to an individual.
CN102805857A Preparation method of compound amino acid (15) dipeptide (2) injecta The invention relates to a preparation method of compound amino acid (15) dipeptide (2) injecta, specifically comprising the following steps of: under the whole-course protection of nitrogen, taking water for injection with a certain quantity, sequentially adding glycyl-L-glutamine, glycyl-L-tyrosine and arginine with prescription quantity, stirring and dissolving, clearly dissolving, adding aspartate, glutamic acid, leucine, isoleucine and phenylalanine with prescription quantity which is not less than 60 screen meshes, dissolving and clearly dissolving, adding alanine, histidine, L-lysine monoacetate, methionine, proline, serine, threonine, tryptophan and valine with prescription quantity, stirring and clearly dissolving, adjusting the pH at 5.4-5.8 by citric acid, adding full dose of 0.10% (w/v) of activated carbon, stirring for 30min under the temperature of 60DEG C, fixing the volume to total volume by the water for injection after filtering in a decarbonizing way, sieving by a filter membrane with 0.22 micrometers, filling, charging nitrogen, adding a plug, pricking an aluminum cap, and sterilizing for 8-12min in a hot-press way under the temperature of 121DEG C (F0 value is larger than 8), wherein the quality of the injecta can achieve the quality standard of an imported drug of the finished product of the German Fresenius Corporation.
CN1887261A Slow released compound anticancer injection containing bendamustine The slow released compound anticancer injection containing bendamustine consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is the composition of bendamustine and bendamustine synergist selected from antitumor antibiotic and antimetabolite. The slow releasing supplementary material is polylactic acid and its copolymer, polifeprosan, EVAc, etc or their composition. The .suspending agent has viscosity of 80-3000 cp. The slow released microsphere may be also prepared into slow released implanting agent. The present invention can inhibit the growth of tumor and enhance the curative effect of chemotherapy, radiotherapy and other non-operative treatment.
WO2013123456A1 Linear peptide antibiotics Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. The compounds provided herein can in other embodiments overcome the resistance conferred by single amino acid mutations at defined positions of bacterial Signal Peptidases (SPases) and in other embodiments provide for a broad spectrum of antibiotic bioactivity. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
US20110021458 Pharmaceutical compositions containing an inclusion complex formed by disulfiram and a cyclodextrine, which can be used in the treatment of alcohol and cocaine dependence The invention relates to a novel pharmaceutical composition containing a complex of disulfiram (DSF) with a cyclodextrin (CD), to the method for obtaining same and to the use thereof in the treatment of alcohol and cocaine dependence.
CA2325471C Piperididinyl and n-amidinopiperidinyl derivatives This invention is directed to a compound of formula (I) which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of formula (I), methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
EP1720837A1 Derivatives of n-' (1,5-diphenyl-1h-pyrazol-3-yl) sulphonamide with cb1 receptor affinity The invention relates to compounds having formula (I), the preparation method thereof and the use of same in therapeutics, wherein: R1 represents a (C1-C6)alkyl, a (C3-C7)cycloalkyl which is unsubstituted or is mono- or poly-substituted, a (C3-C7)cycloalkylmethyl which is unsubstituted or is mono- or poly-substituted, a phenyl which is unsubstituted or substituted; a benzyl which is unsubstituted or is mono- or disubstituted, a thienyl which is unsubstituted or substituted; R2 represents a hydrogen atom or a (C1-C3)alkyl; R3 represents a hydrogen atom or a (C1-C5)alkyl; R4, R5, R6, R7, R8 and R9 each represent, independently of each other, a hydrogen atom, a halogen atom, a (C1-C7)alkyl, a (C1-C5)alkoxy, a trifluoromethyl radical or a S(O)nAlk group; n represents 0, 1 or 2; and Alk represents a (C1-C4)alkyl. The invention also relates to the preparation method thereof and to the use of same in therapeutics.
US6967259 Process for the preparation of Citalopram intermediate The present invention provides, inter alia, a novel process for the preparation of Citalopram, a known antidepressant.
CN102784115A Oral tablet containing iloperidone, and its preparation method The invention discloses an oral tablet containing iloperidone, and its preparation method. The oral tablet is characterized in that the oral tablet contains iloperidone, hydroxypropyl methylcellulose, lactose, microcrystalline cellulose, a disintegrating agent, a lubricant, and a flow aid, wherein the application amount of the hydroxypropyl methylcellulose is 4.0-6.0%. The iloperidone tablet prepared according to the preparation method in the invention has good in-vitro dissolution to guarantee the iloperidone tablet has a good in-vivo biological utilization degree. Simultaneously the invention also provides the preparation method of the oral tablet, and the preparation method has the advantages of simple technology, low cost, and suitableness for commercial production.
CN1837229A Clarithromycin derivatives and its preparation process and pharmaceutical application The invention relates to Clarithromycin derivatives, the preparing process and medicinal use, the Clarithromycin derivatives have general formulas of (I), (II), these compounds and the medicinal compositions of them can be used for treating infectious diseases caused by sensitive organisms and other pathogenic agents.
CN103125627A Smoking cessation tea The invention discloses smoking cessation tea. The smoking cessation tea comprises 18 g of radix pseudostellariae, 10 g of peppermint, 7 g of lumbricus, 12 g of cordate houttuynia, 12 g of polygala tenuifolia, 5 g of sodium bicarbonate and a moderate amount of green tea and brown sugar. The smoking cessation tea enables a smoker to quit smoking easily, relieves smoke toxin and has no toxic and side effect. The smoking cessation tea can enable the smoker to quit smoking thoroughly and has no rebounding effect.
EP1793821A2 Pyrazolone compounds for treating cerebrovascular disorders A drug including edaravone for the treatment of cerebrovascular disorders associated with insufficient cerebral circulation such as ischemic stroke, which comprises a pharmaceutically effective amount of a pyrazolone compound of structural Formula (I): or a pharmaceutically acceptable salt thereof, or a pseudo-polymorphic form thereof, administered at a controlled dose so that the plasma concentration of unchanged form is kept constant for a predetermined period of time and so that the compound may exhibit a higher effect.
EP2402009A1 Inhibitors of serine protease, particularly hepatitis c virus NS3-NS4A protease, incorporating a fused ring system The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.
WO2010050191A1 1,2-diazetidin-3-one derivative and pharmaceutical agent comprising same Disclosed is a novel compound which is useful as a prophylactic or therapeutic agent for diseases associated with 11β-hydroxysteroid dehydrogenase 1 (particularly diabetes, insulin resistance, diabetic complications, obesity, dyslipidemia, hypertension, fatty liver or metabolic syndrome). Specifically disclosed is a 1,2-diazetidin-3-one derivative represented by general formula (1), a salt thereof, or a solvate of the compound or the salt.
US7135465 Sustained release beadlets containing stavudine Extended dosage forms of stavudine are provided comprising beadlets formed by extrusion-spheronization and coated with a seal coating. The beadlets are also coated with a modified release coating such that a hard gelatin capsule containing such beadlets will provide blood levels of stavudine over approximately 24 hours. The beadlets are prepared from a dry blend of stavudine, a spheronizing agent, a suitable diluent and a stabilizing amount of magnesium stearate. The magnesium stearate, in contrast to other similar pharmaceutical adjuncts, has been found to stabilize stavudine against degradation due to hydrolysis in the presence of the limited amount of water necessary for the extrusion-spheronization process. Also included in the scope of the invention are hard gelatin capsules containing, in addition to the stavudine beadlets, similar beadlets containing other therapeutic agents utilized to treat retroviral infections.
US20130035310 Piperidine and Piperazine Phenyl Sulfonamides as Modulators of Ion Channels The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
CN103626741A Heterocyclic aminopyrimidine compound with adenosine receptor antagonist activity The invention provides a heterocyclic aminopyrimidine compound with adenosine receptor antagonist activity. The heterocyclic aminopyrimidine compound with adenosine receptor antagonist activity comprises the compound, pharmaceutically acceptable salts of the compound, various isotopes, various isomers and various crystal structures and has a structure as shown in a general formula I. Serving as an effective antagonist of an adenosine receptor, the heterocyclic aminopyrimidine compound with adenosine receptor antagonist activity can be used for treating or preventing diseases caused by adenosine level disorder.
WO2011041596A2 19-nor-vitamin d analogs with 1,2-or 3,2-cyclopentene ring 19-nor-vitamin D analogs having an additional cyclopentene ring connecting carbon 1 and carbon 2, or connecting carbon 3 and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro activities, making them therapeutic agents for the treatment or prophylaxis of some types of cancers, particularly leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
WO2008104812A2 C21-de0xy ansamycin derivatives as antitumor agents According to the invention there are provided derivatives of a C21-deoxy ansamycin or salt thereof which contain a 1-hydroxyphenyl moiety bearing at position 3 an aminocarboxy substituent, in which position 5 and the aminocarboxy substituent at position 3 are connected by an aliphatic chain of varying length characterised in that the 1-hydroxy position of the phenyl ring is derivatised by an aminoalkyleneaminocarbonyl group, which alkylene group (which may optionally be substituted by alkyl groups) has a chain length of 2 or 3 carbon atoms, a phosphoric acid, or a phosphoric acid ester (such as an alkyl ester) group, or a salt thereof, and which derivatising group increases the water solubility and/or the bioavailability of the parent molecule. Such compounds are useful in therapy eg in the treatment of cancer and B-cell malignancies.
EP1513525B1 Use of mglur5 antagonists for the treatment of gerd The present invention relates to the use of metabotropic glutamate receptor 5 antagonists for the inhibition of transient lower esophageal sphincter relaxations. A further aspects of the invention is directed to the use of metabotropic glutamate receptor 5 antagonists for the treatment of gastro, esophageal reflux disease, as well as for the treatment of regurgitation and asthma.
WO2012044936A1 Combination therapy with 4-(3-(2h-1,2,3-triazol-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing a SYK inhibitor, or a pharmaceutically acceptable salt thereof, and a antineoplastic or antiinflammatory agent for the treatment of inflammatory, autoimmune and cell proliferative diseases, such as allergic reaction, transplant rejection, rheumatoid arthritis (RA), lupus, multiple sclerosis (MS) or psoriasis undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL) (including diffuse large B cell lymphoma (DLBCL)), mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic (SLL), Lymphoma, multiple myeloma, asthma, vasculitis, Idiopathic thrombocytopenic purpura (ITP), Heparin Induced Thrombocytopenia (HIT) and hemolytic anemia.
CN101371826B Percutaneous absorption patch The invention provides a percutaneous absorptive patch, wherein percutaneous absorptive preparation layer composed of copolymer of acrylic acid 2-ethylhexyl of 70 to 80 wt.% and vinyl pyrrolidone of 30 to 20 wt.%, polyethylene glycol mono-hexadecyl ether, n-octanoic acid and/or oleic acid, dodecylic acid diethanol amine, plasmosan and fentanyl, is present on a surface of a backing layer that has no permeability to drugs, in the percutaneous absorptive preparation layer, the weight ratio of copolymer of acrylic acid 2-ethylhexyl of 70 to 80 wt.% and vinyl pyrrolidone of 30 to 20 wt.%, polyethylene glycol mono-hexadecyl ether, n-octanoic acid and/or oleic acid, dodecylic acid diethanol amine, plasmosan and fentanyl (citrate) is 100:1-10:1-10:1-5: 5-20:5-15.
CN102908331A Duloxetine hydrochloride enteric capsules and preparation method thereof The invention relates to the technical field of medicinal preparations, in particular to duloxetine hydrochloride-containing enteric capsules and a preparation method thereof. The enteric capsules consist of capsule shells and coated pellets, wherein the coated pellets also comprise duloxetine hydrochloride-containing medicine carrying pellet cores and coating layers; and the medicine carrying pellet cores contain a disintegrating agent. In preparation of the medicine carrying pellet cores, the duloxetine hydrochloride raw material is subjected to super micronization, so that the particle size distribution that the diameter of 99 percent is not greater than 50 mum, the diameter of 90 percent is not greater than 35 mum, the diameter of 50 percent is not greater than 20 mum and the diameter of 5 percent is not greater than 10 mum is achieved; and after the disintegrating agent is added into the medicine carrying pellet cores, the release speed of the medicine in intestines is increased. According to the duloxetine hydrochloride-containing enteric capsules and the preparation method thereof, a method of directly preparing the medicine carrying pellet cores is adopted, so that the complexity for loading a medicine on blank pellets of the existing domestic and foreign similar products is reduced, the technological process is simplified, and the duloxetine hydrochloride raw material is firstly crushed to a certain particle size range and then prepared into the medicine carrying pellet cores; and the prepared capsules have uniform medicine content and high reproducibility and are suitable for industrial production.
WO2013035833A1 Morphinan derivative A morphinan derivative represented by general formula (I) or an acid addition salt thereof is used as an analgesic. (In the formula, R1 represents a hydrogen atom, a C1-6 alkyl group, a cycloalkyl alkyl group (wherein the cycloalkyl moiety has 3-6 carbon atoms and the alkylene moiety has 1-5 carbon atoms), an aralkyl group (wherein the aryl moiety has 6-10 carbon atoms and the alkylene moiety has 1-5 carbon atoms) or the like; R2 represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a C6-10 aryl group, an aralkyl group (wherein the aryl moiety has 6-10 carbon atoms and the alkylene moiety has 1-5 carbon atoms) or the like; each of R3, R4 and R5 represents a hydrogen atom, a hydroxy group, a carbamoyl group, a C1-6 alkoxy group, a C6-10 aryloxy group or the like; each of R6a, R6b, R7, R8, R9 and R10 represents a hydrogen atom or the like; X represents O or CH2; and Y represents C=O, SO2, a bonding hand or the like.)
US20120263666 Topical skin care composition A cream base for the topical application of skin care therapeutics and a process for making the cream base. In one embodiment, the therapeutic is tretinoin, hydroquinone and fluocinolone acetonide for the treatment of hyperpigmented skin conditions, such as melasma.
WO2007074753A1 Pharmaceutical comprising substituted urea derivative Disclosed is a pharmaceutical comprising an urea derivative having an excellent anorexigenic effect or a pharmacologically acceptable salt thereof as an active ingredient. The pharmaceutical is an anoerxigenic agent and/or an appetite suppressant which comprises an urea derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient. [Chemical formulae 1] (I) (II) (III) (XXXIX) (XL) wherein R1 represents a C6-C10 aryl group which may be substituted at one to five positions independently by a group selected from the substituent group (a) or the like; R2 represents a C6-C10 aryl group which may be substituted at one to five positions independently by a group selected from the substituent group (a) or the like; E represents a group represented by the formula (II) or (III) or the like (wherein R3 represents a hydrogen atom or the like; R4 and R5 independently represent a hydrogen atom or the like; X and U independently represent a group represented by the formula CH or the like; and m and n independently represent 1 or the like); and A represents a group represented by the formula -NH-C(=O)- or the like.
WO2010143919A3 Method and composition for preventing or treating il-6-mediated diseases or rhinovirus infections The present invention relates to a use of Hippophae rhamnoides extract or compounds isolated therefrom for preventing or treating IL-6-mediated diseases or rhinovirus infections. More particularly, the present invention relates to a method and composition which can prevent and treat rhinovirus infections and IL-6-mediated diseases using an extract from Hippophae rhamnoides or quercetin 3-glucoside-7-rhamnoside isolated from the extract, by inhibiting a signal transduction pathway specifically induced by IL-6.
WO2008024974A1 Pyrimidine and pyrazine derivatives Disclosed are compounds and pharmaceutically acceptable salts of Formula (I) wherein R0, R3, R7, n, Q1, Q2, Y, and X1-X3 are as defined herein. Compounds of Formula (I) are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
US20080070954 inhibitors of histone deacetylase; antiproliferative; anticancer; 8-[3-(4-methylbenzenesulfonyl)-ureido])-octanoic acid hydroxyamide The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to acylurea/sulfonylurea containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities.
CN101856325A Hydrochloric acid melphalan injection liquid and preparation method thereof The invention relates to the technical field of medicine preparations. The hydrochloric acid melphalan is very unstable in water, and a large amount of medicine degrades after several hours to generate impurities causing toxic or side effect, so the hydrochloric acid melphalan is not suitable for being prepared into medicine water solution to be stored for a long time. The invention provides stable hydrochloric acid melphalan injection liquid, which consists of hydrochloric acid melphalan, injection-use solvents and pH value regulating agents, wherein the injection-use solvents are anhydrous solvents obtained through dewatering treatment. The hydrochloric acid melphalan injection liquid of the invention has the advantages of stable preparation, low cost, autoclaving capability and small toxic or side effect.
WO2008112479A1 Salts of 3- (1h-ind0l-3-yl) -4- [2- (4-methyl-piperazin-i-yl) -quinazolin-4-yl] -pyrrole-2, 5-di one The invention provides acid addition salts of 3-(1.H.-indol-3-yl)-4-[2-(4-methyl-piperazin-1-yl)-quinazolin-4-yl]-pyrrole-2,5-dione, crystalline forms thereof, processes for the preparation thereof, pharmaceutical compositions comprising them and uses thereof in therapeutic treatment.
CN101002776A Broad-spectrum antibiotic preparation An ointment of the quinolone medicine for treating dermatitis is prepared from the medicine A and emulsion matrix. Said medicine A is 6-fluoro-1-methyl, 4-oxy-7- (1-piperazinyl)-4H-[1, 3] thiazine [3, 2-a] quinoline-3-carboxylate, or its hydrochloride, or its methanesulfonate.
US20120252860 Novel N, N'-Hydrazino-bis-isatin Derivatives with Selective Activity Against Multidrug-Resistant Cancer Cells The invention is directed to a compound of Formula (I), wherein R is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; R1 is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; X is selected from the group consisting of hydrogen atom or halogen atom; and Y is selected from the group consisting of hydrogen atom, halogen atom, C1-C4 alkyl group, nitro group, and —OCF3 group, as well as for its use in therapy, preferably for the treatment of cancer, and to a related pharmaceutical composition, the use of the compound for the manufacture of a medicament for the respective medical indication, and a method of synthesis of the compounds of the invention.
CN101342180A Medicament composition for eyes and preparation method thereof The invention relates to a medicine composite and a preparation method thereof, in particular to an ophthalmic medicine composite and a preparation method thereof. The ophthalmic medicine composite comprises an antivirus medicine with 0.005 to 5.0 weight percent of effective dose, DXM with 0.0005 to 0.1 weight percent of the effective dose and medicinal additive. The medicine composite used for curing herpes simplex keratitis can greatly enhance the recovery process of the herpes simples keratitis and deep solid herpes simples keratitis, effectively improve eye irritation symptoms, shorten healing time and reduce the recurrence rate of the herpes simples keratitis.
CN1813698A Anti-pruritic formulation containing capsaicin, and its preparing method and use The present invention provides an itching-relieving preparation containing capsaicine and its preparation method. Said preparation method is characterized by dissolving capsaicine, menthanol and propanediol in 10-80% ethyl alcohol to make the concentration of capsaicine be 0.03-0.07%, concentration of menthanol be 1-5% and the concentration of propanediol be 15-35%. The invented itching-relieving preparation can be used for making medicine for curing itching and swelling pain due to mosquito bite.
CA2625152A1 Zeolite supported metallic nanodots A metal nanodot material is formed by ion-exchange with an ETS zeolite, followed by activation to form metallic nanodots. The nanodot may be formed from silver, nickel, copper, gold or a platinum group metal.
CN103110640A Pharmaceutical composition of injection ceftizoxime sodium and compound amino acid injection The invention relates to a pharmaceutical composition of injection ceftizoxime sodium and compound amino acid injection and in particular relates to combined application package. The pharmaceutical composition includes injection ceftizoxime sodium and compound amino acid injection. During a using process, the injeciton ceftizoxime sodium is dropped to the compound amino acid injection for intravenous infusion of 30 minutes to 2 hours. For the compatibility mixing of the injection ceftizoxime sodium and the compound amino acid injection, the combined application package disclosed by the invention is used for simplifying the steps and improving the safety. Moreover, the stability of the ceftizoxime sodium is greatly facilitated, and the clinical application quality and the bioavailability of the medicine are improved.
US20100056617 Role of limonoid compounds as neuroprotective agents Disclosed herein are neuroprotective compounds. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of neurodegenerative conditions are provided.
CA2407415C Chondroitin synthase gene and methods of making and using same The present invention relates to a chondroitin synthase gene and methods of making and using same. In more particular, but not by way of limitation, the present invention relates to a chondroitin synthase gene from Pasteurella multocida and methods of isolating and using same. Additionally, the present invention relates to the use of unsulfated chondroitin and its preparation, as well as conversion into modified versions such as dermatan sulfate and chondroitin sulfate polymers.
CN1977858A Special emulsion for treating coppernose The present invention relates to a specific cream for curing rosacea. Its main components include sulfur, 2-naphthol, ethyl alcohol, peanut oil and triethanolamine-stearic acid.
WO2007135941A1 Method for production of acetic acid bacterium-type ceramide [PROBLEMS] To provide a method for efficient production of an acetic acid bacterium-type ceramide which is expected to have physiological activities such as an activity of making the skin beautiful, by increasing the content of ceramide in an acetic acid bacterium. [MEANS FOR SOLVING PROBLEMS] Provided is a method for increasing the content of an acetic acid bacterium-type ceramide, which can increase the content of acetic acid bacterium-type ceramide in an acetic acid bacterium to a level higher by 10 to 30 times than that in an untreated acetic acid bacterium. The method comprises maintaining an acetic acid bacterium after culture at pH 2.0 to 8.0 and a temperature ranging from 4 to 70˚C for a period ranging from 3 hours to 7 days. The acetic acid bacterium used in the method is preferably Acetobacter malorum strain NCI1683 (FERM BP-10595) or Gluconacetobacter hansenii strain NCI1468 (FERM BP-10596).
CN101406547A Facial mask for treating comedo The invention relates to a facial mask for treating acne, which consists of 50 to 60 grams of rhubarb, 20 to 30 grams of scutellaria, 20 to 30 grams of honeysuckle flower, 50 to 60 grams of forsythia, 40 to 50 grams of oldenlandia diffusa, 20 to 30 grams of angelica dahurica, 80 to 100 grams of plaster, 1 to 5 grams of borneol, and 5 to 8 grams of piperitol; the medicaments are screened, mixed and dried, and then crushed, filtered by a sieve of 120 meshes, sterilized, and modulated to pasty mask by warm water at a temperature of between 40 and 60 DEG C. The facial mask can effectively promote pore expansion and promote excrete of sudoriferous glands; therefore, the facial mask is favorable for removing external dust, chemical pollutant and microbe contaminated in the pore, and eliminating waste generated by metabolism of epithelial cells and excessive accumulative fat class materials at the same time; moreover, the treatment medicament of the facial mask is directly acted on pathologic change parts, so as to avoid loss during medicament absorption and metabolism, and improve bioavailability of the medicament remarkably.
CN103372068A Formula and preparation method of novel gold paste The invention discloses a formula and a preparation method of novel gold paste, which relate to the field of medicine formulas for curing skin and surgery diseases and preparation methods thereof. The medicine formula comprises the following constituents: 20%-30% of goldthread root, 30%-40% of nutgall, and 20%-30% of black alum. The preparation method comprises the following steps of: 1, cleaning and drying the goldthread root, the nutgall and the black alum medicine, and milling the goldthread root, the nutgall and the black alum medicine after drying; 2, sieving the medicine powder after milling and auxiliary constituents through a 200-mesh sieve, and uniformly stirring the sieved materials with alcohol, thus obtaining paste suspension; 3, mixing the medicine powder and the auxiliary constituents which are ground into powder; and 4, mixing the mixed powder with alcohol to prepare the paste. The novel gold paste provided by the invention can be used for clearing away heat and toxic materials, removing blood stasis, generating new skin, curing 37 skin surgery stubborn diseases for one time at 3-10 minutes, and naturally repairing shallow dents and bulges on medication points.
WO2012106524A3 Diagnosis and treatment of the prodromal schizophrenic state Described herein are compounds (including medical foods, pharmaceutical compositions, methods of compounding them), methods and systems for the diagnosis and/or treatment of prodromal schizophrenia. For example, described herein are methods of treating a developmentally-based neuropsychiatric disorder (schizophrenia) that includes first determining if a subject is at risk for such a disorder by examining phenotypical, serological immune markers and genotypical biomarkers. The biomarkers may be used to tailor the dose to be delivered by the medial food or pharmaceutical composition. Also described are compounds for treating prodromal (rather than full-blown) schizophrenia.
WO2014007853A1 Dihydromyricetin for the treatment of diseases and disorders of the glutamatergic system Disclosed herein are methods and compositions for treating a disease or disorder of the glutamatergic system, e.g., Alzheimer's disease, neuron damage and/or loss, and seizures, or a symptom thereof, e.g., decreased cognitive function, in a subject which comprises administering dihydromyricetin (DHM), an analog of DHM, or a metabolite of DHM to the subject.
CN102160855A Dex-ibuprofen sustained release tablets and preparation method thereof The invention belongs to the technical field of pharmacy, and in particular relates to a prescription and preparation of dex-ibuprofen sustained release tablets. The dex-ibuprofen sustained release tablets are prepared by mixing a quick release part, a sustained release part and magnesium stearate, wherein the quick release part comprises the following components in part by weight: 40 to 80 partsof dex-ibuprofen, 31.0 to 240 parts of starch, 10.0 to 60 parts of hydroxypropylcellulose, and 1.0 to 5.0 parts of 3 mass percent of hydroxypropyl methylcellulose solution; the sustained release partcomprises the following components in part by weight: 220 to 260 parts of dex-ibuprofen, 10 to 40 parts of microcrystalline cellulose, 40 to 130 parts of hydroxypropyl methyl cellulose and 2.0 to 8.0parts of ethyecellulose; and the magnesium stearate accounts for 3.0 to 18.0 weight parts of the total weight. The dex-ibuprofen sustained release tablets prolong the release time of the medicine in vivo, are easily absorbed by a human body, reduce irritation to gastrointestinal tract and improve the bioavailability.
US20090324537 Polymeric Materials as Stomach Filler and Their Preparation The present invention relates to swellable polymeric materials comprising a synthetic polymer, or copolymer, comprising a carboxylic group and a biopolymer that are suitable for bioapplications. Because of their ability to swell, the polymeric materials are suitable for use as stomach fillers for the treatment of being over weight or obese, or for inducing the feeling of being satiated. Methods for preparing the swellable polymeric materials comprising aqueous reaction systems are also disclosed.
CN102557969A Cyclic ketone derivatives and applications thereof as developers and aggregation inhibitors of amyloid protein sediments and neurofibrillary tangles The invention relates to applications of compounds of formulas (1)-(58), or pharmaceutically-acceptable salts, esters, amides or prodrugs thereof as developers and aggregation inhibitors of amyloid protein sediments and neurofibrillary tangles, a preparation method labeled compounds for imaging, and a method for transporting the compounds to amyloid protein sediments and neurofibrillary tangles. When serving as the developers used to detect the amyloid protein sediments and neurofibrillary tangles in body and tissue, the compounds need to use appropriate radioisotopes or contrast agents suitable for magnetic resonance detection to be labeled. The compounds of the invention are applied to diagnose and treat patients suffering from amyloid protein sediments and neurofibrillary tangles and Alzheimer disease.
CN103570586A D-phenylglycine derivatives, as well as preparation method and use thereof The invention discloses D-phenylglycine derivatives as shown in a formula I. In the formula 1, XR2 is methoxy, and R1 is ethyl, (N-fmoc-amino) methyl and the like; or R1 is chloromethyl, and XR2 is ethoxy, butoxy, N-(2-hydroxyethyl) amino, N-methylamino, N, N-dimethylamino, N-ethylamino, N-propylamino and the like. In the D-phenylglycine derivatives disclosed by the invention, the PPAR (peroxisome proliferator-activated receptor) relative activation activities of five compounds and rosiglitazone exceed 50%, the PPAR relative activation activities of two compounds exceed 100%, the PPAR relative activation activity of a compound TM2-10 is highest (196.47%), and the compounds can be used for preparing a PPAR agonists and are possible to be developed into anti-diabetic new medicaments or be used as anti-diabetic leading molecules for further structure optimization.
US6989387 Topoisomerase inhibitors; use treating cancer, as antifungal agent, treating bacterial infections; compounds based on Dibenzo[c,h][1,6]Naphthyridine ring with at least one nitro or amine-based substitution The invention provides compounds of formula I: wherein R1–R9, W, and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
WO2013119957A1 Weight reduction through inactivation of gastric orexigenic mediator producing cells The present disclosure describes weight loss interventions, including methods of inactivating cells producing appetite inducing stimuli termed orexigenic mediators. Specifically described are compositions and methods for inactivating such cells using photodynamic therapy directed at cells that produce orexigenic mediators.
US20130281515 Cationic bis-urea compounds as effective antimicrobial agents A cationic bis-urea compound is disclosed of formula (1): wherein: each m is independently an integer of 0 to 4, each k is independently 0 or 1, each Z′ is a monovalent radical independently selected from the group consisting of hydroxyl (*—OH), carboxyl (*—COOH), cyano (*—CN), nitro (*—NO2), sulfonate (*—SO3 −), trifluoromethyl (*—CF3), halides, amine groups, ketone groups, alkyl groups comprising 1 to 6 carbons, alkoxy groups comprising 1 to 6 carbons, thioether groups comprising 1 to 6 carbons, and combinations thereof, each L′ is independently a divalent alkylene group comprising 1 to 6 carbons, wherein a *-[-L′-]k- is a single bond when k is 0, each Y′ is independently a monovalent non-polymeric radical comprising a positive charged amine, and each X′ is independently a negative charged counterion.
WO2006077724A1 Cancer vaccine preparation [PROBLEMS] To overcome problems that conventional cancer vaccines can only activate killer T cells or can only activate killer T cells and helper T cells and that there is no practically useful cancer vaccine preparation which is capable of activating antigen-presenting cells as well. [MEANS FOR SOLVING PROBLEMS] A preparation comprising a combination of a complex of a cancer antigen and a hydrophobized polysaccharide with a antigen-presenting cell-stimulating agent which is capable of binding to a Toll-like receptor can activate all of antigen-presenting cells, killer T cells and helper T cells (all of which are major cells involved in the induction and activation of antigen-specific immunity against cancer cells) to exhibit a potent vaccinal effect. The vaccine preparation can evoke immune response to cancer antigens, and particularly has effects of activation and induction of cytotoxic T cells and helper T cells. Therefore, the vaccine preparation can be used as a vaccine for treatment or prevention of cancer.
WO2008138754A3 New solid forms of fxa inhibitors The invention is concerned with crystalline forms or amorphous forms of a pyrrolidine- 3,4-dicarboxamide derivative, which is useful as an active ingredient of medicaments for the diseases which can be treated by the coagulation factor Xa inhibitors.
CN102015662A 3,5-diamino-6-chloro-pyrazine-2-carboxylic acid derivatives and their use as epithelial sodium channel blockers for the treatment of arway diseases A compound of Formula (I) in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
EP2044937A1 ANALGESIC 5, 9 - METHANOCYCLOOCTA (b) PYRIDIN - 2 (1H) - ONE DERIVATIVES, THEIR PREPARATION METHOD AND USE Compounds represented by the Formula I or salts, hydrates thereof, wherein R1, R8, R11 and R12 are H or C1-4 hydrocarbonyl respectively; R2, R3, R6 and R7 are H, halogen or C1-4 hydrocarbonyl respectively; R4 is C1-6 hydrocarbonyl or Ar; or =CR4R3 is cyclopentylidene, cyclohexylidene, 1-methylpiperidyl-4-idene or indenyl-1-idene; R5 is H, 1-4 same or different F, Cl, Br, CF3, R9, OR9, NR9R10, NO2, CN, COOR9, O2CR9, CONR9R10, NR9C(O)R10, heterocyclic, aryl or groups represented by the Formula II respectively; R9 and R10 are H or C1-6 hydrocarbonyl; Ar is aromatic ring; m is 0, 1 or 2; n is 0, 1, 2, 3 or 4, for treating mammal pain, functional painful syndrome, organic painful syndrome or tissue painful syndrome, and their preparation method.
US20120178738 Dibenzo [b,f] [1,4]oxazapine compounds The present invention relates to 11-(piperazin-1-yl)dibenzo[b,f][1,4]oxazapine compounds of the formula: where the variables are as defined herein, their salts and pharmaceutically acceptable compositions thereof. Methods of preparing these compounds are also described. These compounds may be used in the treatment of disorders such as schizophrenia, treatment resistant schizophrenia, bipolar disorder, psychotic depression, treatment resistant depression, schizophrenia-associated depression, treatment resistant OCD, autism, senile psychosis, psychotic dementia, L-DOPA induced psychosis, psychogenic polydipsia, psychotic symptoms of neurological disorders, sleep disorders.
CN102755320A Medicine composition and healthcare food for treating arthritis The invention relates to a medicine composition and healthcare food for treating arthritis. The medicine composition and the healthcare food employ the Antofine or the extractant of the Cynanchum plant as the active ingredients to treat arthritis or as the replenishment to daily diet. The invention also discloses a method for mass production of Antofine via frond.
EP1173163B1 Pharmaceutical compositions of tetrac and methods of use thereof The present invention provides novel pharmaceutical compositions and methods of treatment that utilize or comprise tetrac and/or another thyromimetic compound. The parmaceutical compositions of the invention are capable of suppressing TSH secretion without inhibiting the pituitary specific monodeiodinase type II and while reducing or avoiding the thyromimetic stimulation of peripheral tissues compared to equivalent TSH-suppressive doses of L-thyroxine (T4). The pharmaceutical compositions of the invention are particularly useful for treating patients suffering from malignancy or abnormal growth of the thyroid and for preventing growth of residual thyroid tissue post thyroidectomy.
CA2351273C Solution of n-[o-(p-pivaloyloxybenzenesulfonylamino) benzoyl] glycine monosodium salt tetra-hydrate and drug product thereof A solution of N-[o-(p-pivaloyloxybenzenesulfonylamino) benzoyl]glycine monosodium salt tetra-hydrate (I) comprising at least one pH adjuster selected from tri-sodium phosphate, a hydrate thereof, sodium hydroxide or potassium hydroxide and a drug product using the solution. According to the invention, the solubility of the compound (I) increases and thereby it is possible to provide a solution thereof and a drug product using it. Moreover, by using a mixture of water and an organic solvent, greatly improved solubility makes it possible to manufacture a solution of higher concentration of the compound (I), and high-dosage drug products using it.
EP1917962A1 Pharmaceutical composition for modified release insulin sensitiser This invention relates to a novel composition, in particular to a modified release composition and its use in medicine, especially its use for the treatment of diabetes mcllitus, preferably Type 2 diabetes, and conditions associated with diabetes mcllitus.
EP1703913A2 Use of ribose in recovery from anaesthesia D-Ribose is administered before and after general anaesthesia to reduce the time to recover from the effects of general anaesthesia. Preferably, pyrogen-free D-Ribose is administered intravenously during general anaesthesia and the interval post-anaesthesia before oral administration can be resumed. D-Glucose may be co-administered to reduce the effect of hypoglycemia that may be seen with D-Ribose administration.
CN101234079A Azithromycin ophthalmic gel preparation composition and preparation and application thereof The invention discloses a novel composition of an ophthalmic Azithromycin gel preparation, a preparation method thereof and applications thereof. The researcher of the invention combines appropriate auxiliary materials with the combination of Azithromycin and citric acid to prepare the ophthalmic Azithromycin gel preparation; the combination of the Azithromycin and the citric acid in the invention can achieve better absorption of the Azithromycin, which resolves the problem that the Azithromycin is difficult to dissolve; meanwhile, the manufactured gel preparation can ensure that the drug have prolonged effects on lesion location to realize full absorption of the drug. The ophthalmic Azithromycin gel preparation of the invention has obvious pharmacological action and outstanding effects on treatment of such ophthalmic diseases as conjunctivitis, keratitis, trachoma, dacrocystitis, etc.
WO2009110612A1 New compound derived from germinated brown rice, and agent containing said compound as an active ingredient for prevention or amelioration of neuropathy The purpose of the present invention is to find a new function for a component contained in germinated brown rice, and to provide an effective agent for preventing or ameliorating neuropathy or diabetic neuropathy, or a functional food product, that is highly safe, can be taken continually, can be produced in large quantities, and can be easily added to food products and the like. Provided is an agent for preventing or ameliorating neuropathy or diabetic neuropathy, or a functional food product, that contains as an active ingredient a steryl glucoside (acylated steryl-β-glucoside (ASG)) derived from germinated brown rice.
CN101787022B Quinoline carboxylic acid hydrochloride-hydrate novel crystal form, and preparation method thereof The invention relates to a quinoline carboxylic acid hydrochloride-hydrate novel crystal form, a preparation method thereof and a drug combination applying the quinoline carboxylic acid hydrochloride-hydrate novel crystal form as active compound. The dissolubility of the prior quinoline carboxylic acid is poor, so the prior quinoline carboxylic acid is not suitable for the preparation of stable pharmaceutical preparations. The quinoline carboxylic acid hydrochloride-hydrate novel crystal form shows characteristic diffraction peaks at the positions of 8.0 plus or minus 0.2 degrees, 9.6 plus orminus 0.2 degrees and 12.4 plus or minus 0.2 degrees on an X-ray powder diffraction pattern represented by a 2 Theta diffraction angle. The novel crystal form has high stability, particularly during storage under a high-humidity condition; and the novel crystal form is applicable to the preparation of various forms of drugs, in particular to the preparation of tablets and injections.
US20090306076 Morpholine Carboxamide Prokineticin Receptor Antagonists The present invention is directed to morpholine carboxamide compounds which are antagonists of prokineticin receptors, in particular antagonists of prokineticin 2 receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which prokineticin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which prokineticin receptors are involved.
US20100322989 Hydrophilic skin cleaning cloth A preferably single-ply, simply and inexpensively manufacturable hydrophilic skin care tissue for disposable use comprising a textile surface (1) of microfibres is described. The textile surface (1) has run through a splitting process and comprises a plurality of barbs (14) and accordingly has an abrasiveness with which a micro-dermal abrasion of the facial skin of a user may be carried out. A defined quantity of at least one active ingredient (2) is stored in a mechanically held manner in the textile surface (1) on bows, microfibres and/or grid intermediate spaces (11). The at least one active ingredient is released from the inside of the textile surface (1) by way of the mechanical deformation, and by way of this gets to the pre-treated skin of the user.
CN101953798A Spray drying sustained-release liquid crystal nano particles containing paeonol and preparation thereof The invention relates to spray drying sustained-release liquid crystal nano particles containing paeonol and a preparation method thereof. The nano particles comprise 100 weight parts of active paeonol ingredient, 500 to 5,000 weight parts of glyceryl monooleate, 20 to 100 weight parts of surfactant and 1,000 to 10,000 weight parts of carrier. The spray drying sustained-release liquid crystal nano particles containing the paeonol have obvious sustained-release effect compared with common tablets, and remarkably improve the oral administration bioavailability.
CN102068418A Sofalcone sustained-release pellet capsule preparation and preparation method thereof The invention relates to a sofalcone sustained-release pellet capsule preparation and a preparation method thereof. The capsule preparation comprises the following components in percentage by mass: 30 to 50 percent of sofalcone, 30 to 50 percent of Celphere, 5 to 15 percent of hydroxy propyl methyl cellulose or povidone, 5 to 15 percent of ethyl cellulose or acrylic resin, 1 to 8 percent of talcpowder, 0.5 to 2 percent of colloid silicon dioxide. The preparation method comprises the following steps of: coating raw material fine powder onto the Celphere by using an adhesive to prepare medicated pellets; coating the medicated pellets by using an isolating layer; coating a sustained-release coating membrane onto the medicated pellets coated with the isolating layer to prepare sustained-release pellets; and mixing the sustained-release pellets, the talcpowder and the colloid silicon dioxide and filling the mixture into a capsule. The sofalcone is prepared into the sustained-release capsule preparation by pellet and sustained-release technology, so that the stable plasma concentration of the sustained-release preparation can be achieved, the frequency and the degree of side effects arereduced, medicine taking frequency is reduced, and the problems that tablets are greatly influenced by gastric pyloric sphincter and gastric emptying individual differences are large can be fundamentally solved.
WO2011107903A1 Highly pure mosapride citrate dihydrate and processes for its preparation The present invention provides for highly pure mosapride citrate dihydrate and processes for its preparation. The present invention further provides a process for the preparation of mosapride citrate dihydrate substantially free of impurity D-II.
US8613948 Treatment of faecal incontinence and other conditions with 1R, 2S-methoxamine 1R,2S-Methoxamine may be used topically for effective treatment of faecal incontinence at low doses without local or systemic side effects, for example, without affecting blood pressure. 1R,2S-Methoxamine may be used to treat other disturbances and disorders of the gastro-intestinal, as a pressor agent, as a nasal decongestant and in ophthalmology, at low does and without significant side effects.
US20080242604 Nucleotide sequence coding protein; for therapy of periodontal disease; wound healing agent The present invention relates to novel Nodal and Lefty proteins which are members of the TGF-β family. In particular, isolated nucleic acid molecules are provided encoding the human Nodal and Lefty proteins. Nodal and Lefty polypeptides are also provided as are vectors, host cells and recombinant methods for producing the same. The invention further relates to screening methods for identifying agonists and antagonists of Nodal and Lefty activity. Also provided are diagnostic methods for detecting cell growth and differentiation-related disorders and therapeutic methods for treating cell growth and differentiation-related disorders.
CN103006603A solid dispersion and solid preparation of ulipristal acetate The invention discloses solid dispersion of ulipristal acetate which is prepared from 1 part by weight of ulipristal acetate and 3-20 parts by weight of auxiliary material, wherein the auxiliary material is one or combination of more than two selected from lactose, mannitol, sorbitol and povidone. The invention also discloses a solid preparation of the ulipristal acetate which is prepared from the solid dispersion of the ulipristal acetate and the conventional preparation auxiliary material, wherein the conventional preparation auxiliary material comprises filler, a disintegrating agent, a binding agent, a lubricating agent or flow aid. The solid preparation of the ulipristal acetate disclosed by the invention has higher dissolution rate compared with the ulipristal acetate tablet disclosed by the Chinese patent with the publication number of CN102245173A, the dissolution rate of the ullipristal acetate in a slightly soluble medium can be greatly increased, further bioavailability of the ulipristal acetate is improved and a pharmaceutical effect is guaranteed.
US20110280829 Low Molecular Weight Sulphated Polysaccharides as Candidates for Anti-Angiogenic Therapy Low molecular weight sulphated L-fucose polysaccharide fraction having a molecular weight ranging from 11 to 30 kDa when measured with TEST A, a sulphate content ranging from 10 and 50% w/w relative to the total weight of the fraction, a fucosis content ranging from 30 and 70% w/w relative to the total weight of the fraction, and a polydispersity index ranging from 1 and 2, wherein the fraction is obtainable by free radical depolymerisation of a crude fucan of vegetal origin; process for manufacturing same; pharmaceutical composition and medicament containing same and their use for inhibiting neovascularisation.
CN101011386A Dropping pill of coumarin derivative and its preparation and application Disclosed is a dripping pill medicament containing 6, 7-dimethoxycoumarin and/or 6-hydroxy-7-methylcoumarin, the process for preparation and its use in preparing liver-protection pharmaceuticals.
EP1715843A1 Combination of a nmda receptor antagonist and a mao-inhibitor or a gadph-inhibitor for the treatment of central nervous system-related conditions The invention provides methods and compositions comprising a NMDA receptor antagonist once a monoamine oxidase (MAO) inhibitor GADPH inhibitor for the treatment dementia-related conditions, such as Parkinson’s disease and Alzheimer’s disease.
US20100234416 Use of huperzine for disorders Methods and compositions containing huperzine are used to prevent and alleviate neuropathic pain. The invention is also directed to methods and compositions for using huperzine for the prevention and/or treatment of neuropathic pain and orthostatic hypotension.
CN101991565A Application of salvianolic acid A in preparing medicament for inducing apoptosis of tumor cells and/or inhibiting propagation of tumor cells The invention discloses application of salvianolic acid A in preparing a medicament for inducing apoptosis of tumor cells and/or inhibiting propagation of tumor cells. The application is characterized by discovering that the salvianolic acid A has the characteristics of selectively inducing apoptosis of tumor cells and/or inhibiting propagation of tumor cells without damaging normal cells of a human body, and has remarkable influence on disintegrating related protein. Therefore, the salvianolic acid A can be used as a lead compound of anti-tumor medicaments, and has the application prospect in preparing the medicament for inducing apoptosis of the tumor cells and/or inhibiting propagation of the tumor cells.
US20120142702 Integrin-linked kinase inhibitors A number of compounds and use of the compounds in a method for treating or preventing cancer in a subject by administering to the subject a pharmaceutical composition including a compound of formula I or a pharmaceutically acceptable salt thereof are described. The compounds can also be used to inhibit integrin-linked kinase in a cell, which has an effect on the Akt signaling pathway.
US20050004136 Novel amidoalkyl-piperidine and amidoalkyl-piperazine derivatives useful as neurokinin receptor modulators Novel amidoalkyl-piperidine and amidoalkyl-piperazine derivatives of the general formula wherein all variables are as described herein, useful in the treatment of disorders, such as depression, dementia, schizophrenia, bipolar disorders, anxiety, emesis, acute or neuropathic pain, itching, migraine and movement disorders.
CN101239056A Application of NF-kB inhibitor in treating a plurality of diseases The invention relates to an application used for curing diseases by utilizing NF-kappa B inhibitor and belongs to the applying field of the chemical complex in curing the diseases. The invention regards NF-kappa B as the target, uses the applications of the NF-kappa B inhibitor to cure the virus infection, cancer, chronic inflammation and self-immunological disease when curing the curing mammals. The used inhibitors including that: phenmiazine ramification, oriental biter weed pure, phenethyl caffeate, (E)3-[(tetramethylbenzene)sulfuryl]-2-acrylonitrile, 7-anisyl-5, 11, 12- trihydroxy benzene-Fluindarol and other chemical complexes have NF-kappa B suppressing function as well as the ramification and can be joined with the current therapy applied in the clinical so as to cure virosis, in particular the virus infection caused by the retravirus and AIDS caused by HIV, cancer, chronic inflammation and self-immunological disease.
CA2843805A1 Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament The present inventions relates to substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl- methanones of general formula (I) wherein R1, R2, R3, R4, R5 and R6 are as herein described or salts thereof, preferably pharmaceutically acceptable salts thereof. The invention further relates to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various conditions such as conditions concerning positive and negative symptoms of schizophrenia as well as cognitive impairments associated with schizophrenia, Alzheimers Disease and other neurological and psychiatric disorders. The compounds of the invention show glycine transporter-1 (GlyT1) inhibiting properties.
CN103479674A Intra-gastric floating type cuttlebone sustained release tablet for treating gastric ulcer and preparation method thereof An intra-gastric floating type cuttlebone sustained release tablet for treating gastric ulcer is prepared from the following raw materials: cuttlebone, nano-montmorillonite, hydroxypropyl methyl cellulose, octadecanol, microcrystalline cellulose and magnesium stearate. Compared with the prior art, the sustained release tablet overcomes the defect that the residence time of a common oral preparation drug at the nidus part is short. The intra-gastric floating type sustained release preparation is prepared, so that the reaction rate of calcium carbonate in the cuttlebone and gastric acid can be slowed down as far as possible, and the hyperacidity relief and pain relief time is prolonged. The prepared intra-gastric floating tablet can stay in the stomach for 6-8 hours, so that the release of the tablet is delayed and the absorption is increased. The medicine taking frequency is reduced, and the bioavailability is improved. In addition, the cuttlebone is selected from edible animals of a natural marine, so that the advantages that no toxic or side effects are caused, the safety is high and the like are achieved.
US20070010476 Therapy and diagnosis of conditions related to telomere length and/or telomerase activity Method and compositions are provided for the determination of telomere length and telomerase activity, as well as the ability to inhibit telomerase activity in the treatment of proliferative diseases. Particularly, primers are elongated under conditions which minimize interference from other genomic sequences, so as to obtain accurate determinations of telomeric length or telomerase activity. In addition, compositions are provided for intracellular inhibition of telomerase activity and means are shown for slowing the loss of telomeric repeats in aging cells.
CA2414774C Use of dopamine d2/d3 receptor agonists to treat fibromyalgia The present invention is directed to methods for the treatment of human patients afflicted with fibromyalglia using a non-ergot dopamine receptor D2/D3 agonist. In particular, patients are treated with a therapeutically effective amount of tetrahydro-benzthiazole or 3(H)-indolone compounds that are dopamine agonists. More specifically, the compounds 2-amino-6-n-propylamino-4,5,6,7-tetrahydrobenzo-thiazole or 4-[2-(dipropylamino)-ethyl]-1,3-dihydro-2H-indol-2-one are administered to fibromyalgia patients to reduce the musculoskeletal pain symptoms associated with fibromyalgia.
CN103524372A Novel histone deacetylase inhibitor The invention discloses a novel histone deacetylase inhibitor which is a compound shown in a formula (I) or a pharmaceutical acceptable salt thereof. The compound disclosed by the invention can be applied to the aspect of preparing medicaments for preventing and/or treating diseases relevant to the activity out-of-control of histone deacetylase.
CN1864691B Use of compound scalarafuran The present invention discloses one kind of compound, citiofuran. The compound, citiofuran has very high combination activity, KD=16.4 microM, with HIV-1 integrase, and effective inhibition of the combination of the integrase to the substrate, IC50=120 microM, in substrate competition test. Therefore, the compound exhibits very high medicine preparing value.
US7872037 (4-Isopropyl-benzyl)-[1-(4-methoxy-phenyl)-1H-benzimidazol-5-yl]-amine; potent inhibitor of viral infection mediated by envelopes of the New World arenaviruses Guanarito & Tacaribe; compounds may have utility for treatment of arenavirus diseases other than Lassa fever;hemorrhagic fevers; vaccines Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pichinde, and LCMV), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
CN101278906A Stable lornoxicam solution agent, preparation method and application thereof The invention relates to stable lornoxicam solution and a preparation method and an application thereof; the solution contains the lornoxicam or the pharmaceutically-acceptable salt of the lornoxicam, meglumine, potassium phosphate salt and/or sodium phosphate salt, and has the advantages of good solubility, good stability and good security. The solution of the invention is suitable for parenteral administration such as intramuscular injection, intravenous injection or ophthalmic purpose; the solution which is suitable for the invention is selected from injection preparation, lyophilization formulation or spraying desiccant, preferably the lyophilization formulation.
US20120178787 Melatonin and its use in preventing postoperative complications The invention relates to the use of melatonin, either alone or in combination with at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof, for the manufacture of a medicament for the therapeutic treatment, prophylactic treatment and/or prevention of postoperative infectious and/or non-infections complications induced by surgical interventions wherein the infectious complications may be pneumonia, wound infection (wound dehiscence), intra-abdominal abscess, and urinary tract infections (UTI) or wherein the non-infectious complication may be anastomotic leak, a pharmaceutical formulation comprising melatonin and at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof and a method for the therapeutic and/or prophylactic treatment of postoperative infectious and/or non-infectious complications induced by surgical interventions.
WO2008080092A8 Compositions comprising bile acid sequestrants for treating esophageal disorders Disclosed herein are novel compositions for treating or preventing upper GI tract disorders and protecting stratified squamous epithelium against injury by a noxious substance. The pharmaceutical composition comprises at least one bile acid sequestrant, alone or in combination with at least one proton pump inhibitor, and optionally one or more agent chosen from antacids, histamine H2-receptor antagonists, -aminobutyricacid-b (GABA-B) agonists,, prodrugs of GABA-B agonists, and protease inhibitors.
WO2007135529A3 Azabenzimidazolyl compounds as mglur2 potentiators Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R17, R2, X4, X9, X5, X6, R8, X2, Y1 and n are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
EP1897880A1 1,3-benzothiazinone derivative and use thereof The present invention provides compounds represented by formula (I): wherein R1 independently represents a halogen atom, hydroxy, nitro, an optionally halogenated alkyl, alkenyl or alkynyl, an optionally substituted alkoxy, an acyl, or an optionally substituted amino; R2 represents hydrogen atom or an optionally substituted hydrocarbon group; R3 represents an electron-withdrawing group; n represents an integer of 0 to 2; and m represents an integer of 1 to 6 (hereinafter sometimes briefly referred to as Compound (I)); or salts thereof. These compounds are capable of binding to macrophage migration inhibitory factor (MIF) and useful as agents for preventing/treating diseases induced by oxidative stress.
CN101966263A SOD (Super Oxide Dlsmutase) oxidation-resistant health product The invention relates to an SOD (Super Oxide Dlsmutase) oxidation-resistant health product which is prepared from the following components in parts by weight: 50 to 90 of grape seed extracts, 30 to 60 of natural VC, 45 to 60 of spirulina platensis extracts and 45 to 60 of inonotus obliquus extracts. The SOD oxidation-resistant health product has the synergistic effect of all the components, is rich in the antioxidation of SOD and has free radical balancing and anti-aging function. The SOD contained in the preparation has the advantages of maintaining longer survivability, enhancing antioxidation capacity, eliminating excess oxygen free radicals, regulating lipid metabolism in the human body, preventing the increase of serum total cholesterol and triglycerides, protecting cardiac and cerebral blood vessels, enhancing and improving human body immunity capacity and having more SOD activity units in finished products.
US20120101101 Therapeutic agent for motor disorders Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.
US20110086035 Immunotherapeutic methods and molecules A peptide of less than 10 000 molecular weight comprising the amino acid sequence FHTYTI DWTKDAVTW or a portion thereof, or a variant thereof wherein the side chains of one or two of the amino acid residues are altered, wherein the portion or variant is capable of binding HLA-DRB1*04. The peptide, certain polypeptide fusion molecules and certain polynucleotides encoding the same may be useful in combating Aspergillus infection or allergies. In particular, they may be used in processes for preparing Aspergillus-specific T cells for adoptive immunotherapy.
US20110034543 DNA Vaccination For Treatment of Multiple Sclerosis and Insulin-Dependent Diabetes Mellitus A pro-inflammatory T cell response is specifically suppressed by the injection into a recipient of DNA encoding an autoantigen associated with autoimmune disease. The recipient may be further treating by co-vaccination with a DNA encoding a Th2 cytokine, particularly encoding IL4. In response to the vaccination, the proliferation of autoantigen-reactive T cells and the secretion of Th1 cytokines, including IL-2, IFN-γ and IL-15, are reduced.
WO2007066423A1 Tumor antigen peptide derived from amacr The invention relates to a peptide which contains a partial peptide derived from AMACR and binds to an HLA antigen thereby being recognized by CTL, a pharmaceutical composition containing the peptide and a pharmaceutically acceptable carrier, etc.
EP1224168B1 Antifungal enediynes The invention features enediynes and methods for their production and use. The enediynes of the invention have the formula (I) wherein R1 is a hydroxyl group or a moiety that can be replaced by a hydroxyl group in a hydrolysis reaction; each R2 is, independently, H or a monovalent hydrocarbon moiety containing between 1 and 4 carbon atoms, inclusive; R3 is a pyrrole, furan, or thiophene ring; and X is an integer between 4 and 10, inclusive.
US20130084543 Thiol-ene polymerization with vinylesters and vinylcarbonate The present disclosure is directed, in part, to a curable composition, a method for augmenting a structure in a patient with a resorbable biocompatible polymer, and a biodegradable, resorbable implant comprising a biocompatible copolymer. An exemplary embodiment of the curable composition comprises (a) 60 wt. % to 95 wt. % of one or more vinyl ester monomers and/or vinylcarbonate monomers, wherein said one or more vinyl ester monomers and/or vinylcarbonate monomers are respectively selected from compounds of the general formulas (I) and (II) below: wherein n, m R1 and R2 have the meaning defined herein; (b) 0.1 to 40 wt. % of one or more multifunctional thiols; and (c) 0 to 10 wt. % of a biocompatible polymerization initiator.
US20050049293 Increasing effect of released acetylcholine on hepatic muscarinic receptors There is provided a method of reducing insulin resistance in a mammalian subject comprising administering a suitable acetylcholine esterase antagonist.
US20130217773 Method and Device for assistance in delivery of medication, and Formulas This invention is designed for the convenient and reliable delivery of predetermined doses of topical therapeutic medications applied to the skin. The importance of this method of application is that it allows reducing the amount of a therapeutic agent used in one session or reducing amount of sessions per day by eliminating the application of medications to a treating surface by hand. The emphasis is on making therapeutic agents available for self-administration, especially for partially disabled people with conditions such as arthritis and/or visual impairments who would not be able to use these medications without assistance.
CN1947706A Slow-release, controlled-release prepn. contg. chlortenozicam A slow-release or release-controllable lornoxicam with durable antalgic and anti-inflammation effect is disclosed. The povidone, polyethanediol and poloxamer are used to prepare the dispersing substance of lornoxicam or the beta-cyclodextrin or its derivative is used for preparing its inclusion substance. The slow-releasing material is used for controlling its release.
EP1440071B1 Imidazopyridine compounds as 5-ht 4? receptor modulators This invention provides a compound of the formula (I), or the pharmaceutically acceptable salts thereof wherein R1 is hydrogen, halo or alkyl; R?2 and R3¿ are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R?2 and R3¿ taken together with the nitrogen atom to which they are attached may form hetrocyclic; R4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R5 is hydrogen, halo, alkyl, alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R6 is hydrogen, alkyl or alkoxyalkyl; X is NR9 wherein R9 is hydrogen or alkyl; and Y is (CR7R8) wherein n is an integer from 0 to 5. These compounds have 5-HT¿4? receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, Functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
WO2014078956A1 The use of bucillamine in the treatment of gout Disclosed are pharmaceutical compositions comprising, bucillamine, including bucillamine and allopurinol or colchicine, or pharmaceutically acceptable salts or solvates thereof, together with one or more pharmaceutically acceptable carriers, diluents and excipients. Methods for use of the said compositions in the treatment of gout and metabolic syndrome are also disclosed.
US20080249030 Age Inhibitors The invention relates to a compound having general formula I, wherein: X represents CH2, C═O, C═S or CHOH, X represents CH2, C═O, C═S or CHOH, R1 represents an amino acid which is optionally substituted by one or more halogen atoms, preferably fluorine, or by one or more CF3 groups and n=0.1 or 2, or X represents CH2, C═O, C═S, CHOH, R1 represents a peptide containing two amino acids, each amino acid being optionally substituted by one or more halogen atoms, preferably fluorine, or by one or more CF3 groups and n=0 or 1, or XR1 represent PO3H or SO3H and n=0.1 or 2; R2 represents H, XR1, an alkyl group at C1-C6, an aralkyl group at C1-C6 or an aryl group, whereby the alkyl, aralkyl and aryl groups can be substituted by an amine NH2, a carboxylic group COOH, one or more halogen atoms, preferably fluorine, or one or more CF3 groups; or the pharmaceutically-acceptable addition salts, isomers, enantiomers and diastereoisomers of said compound, mixtures thereof, and pharmaceutical or cosmetic compositions comprising same and the use thereof as an AGE-inhibitor drug that traps reactive carbonyl compounds.
EP1126863B1 Vascular endothelial growth factor-like protein from orf virus nz10 binds and activates mammalian vegf receptor-2 The invention is based on the discovery that a viral VEGF-like protein from the orf virus strain NZ2 and from the orf virus strain NZ10 is capable of binding to the extracellular domain of the VEGF receptor-2 to form bioactive complexes which mediate useful cellular responses and/or antagonize undesired biological activities. Disclosed are methods which stimulate or inhibit these biological activities, methods for therapeutic applications and antagonists of ORFV2-VEGF and/or NZ10.
CN103505733A Oral liquid preparation with macrolides medicine as active component The invention discloses an oral liquid preparation with a macrolides medicine as an active component. The oral liquid preparation is characterized by comprising the macrolides medicine, a stabilizing agent, solubilizer, a pH regulating agent, flavoring agent and water. The oral liquid preparation has the active advanced effects of preparing the unstable macrolides medicine into the oral liquid preparation, guaranteeing the consistency of bioavailability, largely reducing the risk in clinical application and ensuring the clinical effect.
CN101690823A Method for preparing RGDV-containing cytosine arabinoside conjugate pharmacosome and application as antitumor agent The invention discloses a method for preparing an RGDV-containing cytosine arabinoside (Ara-C) conjugate pharmacosome and application as an antitumor agent. In the invention, the N4 locus of the cytarabine is connected with a tetrapeptide segment which contains an RGDV sequence, simultaneously, is combined with fatty acids with different lengths so as to synthesize a series of amphipathic Ara-C conjugates; the series of amphipathic Ara-C conjugates are prepared into a pharmacosome; the Ara-C is targeted to a tumor position better by the dual functions that the pharmacosome has a good targeting function and the RGDV serves as a bonding locus for integrating an acceptor. The invention evaluates the antitumor activity of conjugate pharmacosome preparations of Ara-C series by taking a sarcoma S180 mouse as a model, and the result shows that the conjugate pharmacosome preparations of the Ara-C series has more excellent anti-tumor activity than each control group.
WO2011067501A1 Local topical application aminosteroid compounds for mucous/cutaneous decolonization of staphylococcus aureus The present invention relates to the use of a compound selected from among squalamine, or an aminosteroid compound analogous to squalamine, for local topical application for mucous/cutaneous decolonization of Staphylococcus aureus, said squalamine-analogous aminosteroid compound having a general formula that includes a skeleton of Formula (I) below, onto which at least one -NHR polyamine chain is grafted, R being an optionally substituted hydrocarbon chain comprising at least one - NH2 group.
US7033588 combination of coenzyme Q and a surfactant can prevent ascites even when administering in a small dose and within a short period of time It is intended to provide a preventive agent for ascites containing coenzyme Q which can sufficiently exert an effect on preventing ascites even when administering in a small dose and within a short period of time, and the preventive agent for ascites which can be effectively administered to poultry using a simple method. Namely, preventive agent for ascites in poultry containing coenzyme Q and a surfactant, wherein the content of the surfactant is in a range of between 0.5 and 80 parts by weight with respect to a total amount of the preventive agent for ascites.
WO2008034202A3 Use of ivermectin and derivates thereof for the treatment of amyotrophic lateral sclerosis Present invention is directed to a novel medicament for medical treatment of motor neuron disease (NMD) such as amyotrophic lateral sclerosis. More particularly the present invention involves the use of ivermectin and analogues, to prevent, retard and ameliorate a motor neuron disease (MND) such as amyotrophic lateral sclerosis (ALS) and the associated motor neuron degeneration.
US20080131525 Glutamine as a short chain peptide (e.g. dipeptide), and antioxidant selected from selenium, vitamin C, zinc or vitamin E and beta-carotene; parenterally delivered to a critically ill patient for improving mitochondrial function The invention may be summarized as follows. A combination to be parenterally delivered to a critically ill patient or for the purpose of improving mitochondrial function. The combination comprises a glutamine precursor molecule and an antioxidant in sufficient concentrations to be clinically effective. The combination may be prepared in the absence of lipids or carbohydrates. The combination may be prepared in small volumes to benefit volume restricted patients. A composition, or a unit dosage form comprising the combination and methods of administering the combination, composition or unit dosage form are also provided.
CA2386627C Hydroxyeicosatetraenoic acid analogs and methods of their use in treating dry eye disorders Hydroxyeicosatetraenoic acid analogs and methods of their use in treating dry eye disorders are disclosed.
CN1768750A Palonosetron lyophilized formulation and its preparation method The invention relates to the freeze-dried preparation of Palonosetron or its medicinal salts, in particular Palonosetron hydrochloride freeze-dried preparation and its preparing process, which can improve the preparation stability.
CN101245077B Novel cephalosporin derivatives The invention belongs to the technical field of medicine, in particular to a novel cephalosporin derivative shown is the general formula (I), the pharmacologically acceptable salt, the easily hydrolysable ester, the isomer, the hydrate, and the hydrate of the ester or the salt; wherein, R<1>, R<2>, R<3>, R<4> and X are defined in the instruction book; the invention further relates to the preparation methods of the compounds, the medicine combinations containing the compounds, and the application of the compounds in the preparation of medicines for treating and/ or preventing infectious diseases.
WO2009101345A1 Novel anti-infectious derivatives, method for the production thereof, pharmaceutical compositions containing same and uses of said derivatives in treatment The invention relates to bi-substrate inhibitor molecules associating (i) a pyridine, pyridinium or dihydropyridine-type structure allied to active metabolites of isoniazide, or related structures, and (ii) a hydrophobic substituent. The invention also relates to the method for producing said molecules, to the pharmaceutical compositions containing said molecules, and to the use thereof as inhibitors of enoyl reductase for the preparation of a medicament, especially an anti-infectious medicament for the treatment of tuberculosis.
WO2014010656A1 Superior blood alcohol concentration reduction accelerating agent Provided is a blood alcohol concentration reduction accelerating agent which rapidly improves various unpleasant symptoms caused after alcohol consumption such as bloating, nausea and hangover. The blood alcohol concentration reduction accelerating agent is obtained by adding piperine or a piperine-containing crude drug to a preparation.
CN1847258A A-decarbon-5 alpha-androstane-2-one-17 beta-alcohol ester and its prepn and use The present invention relates to A-decarbon-5alpha-androstane-2-one-17beta-alcohol ester possessing PPARalpha/beta/gamma triple excitant activity. The preparation process of the sterides includes the esterification between substituted phenoxy acetyl chloride or substituted nicotine chloride and 17beta-hydroxy-A-decarbon-5alpha-androstane-2-one in the molar ratio of 1.5-2 inside solvent pyridine under the presence of catalyst 4-dimethylin pyridine at reaction temperature of -7 to 10 deg.c for 0.25-12 hr. The present invention has the features of simple operation, high yield, high product purity, etc. and the prepared sterides may be used as type II diabetes treating medicine clinically.
CN101342177B Lornoxicam double-layer sustained release tablets The invention relates to a double-layer sustained release lornoxicam tablet which comprises (a) a quick release layer and (b) a sustained release layer, wherein, the quick release layer comprises (a1) the lornoxicam, (a2) alkaline matter and (a3) an other optional carrier or pharmaceutically acceptable excipient and the sustained release layer comprises the (b1) lornoxicam, (b2) sustained releasesubstance and (b3) the other optional carrier or the pharmaceutically acceptable excipient. The weight proportion of (a1) and (b1) is 1:50 to 50:1. The invention also provides a preparation method ofthe double-layer sustained release lornoxicam tablet. The double-layer sustained release preparation of the invention has the advantages of the quick effect of the quick release preparation and the sustained effect of sustained release preparation. In addition, the double-layer sustained release preparation can maintain the effect of effective blood concentration continuously and stably after theeffective blood concentration is reached rapidly.
US20050013876 Inactivation of papillomavirus A method of treating early papillomavirus infection of an orifice of a human or animal body including any canal associated with an orifice, comprising applying a viral inactivation agent to the orifice and/or canal in an amount effective to inactivate a portion of the virus infecting the orifice or canal. Apparatus is also disclosed.
EP1560573B1 Use of n,n-dicylcohexyl-2-hydroxy-7,7-dimethylbicyclo[2.2.1]hept-1-ylmethanesulfonamide family members in therapy Compositions and methods of using an MT103 family member, wherein MT103 is the chemical N,N-dicyclohexyl-(1s)-isoborneol-10-sulfonamide. Uses of the compositions include cancer therapy, antibacterials, antifungals, induction of apoptosis, and hormonal antagonists.
CN101953834A Formula and preparation process of aztreonam for injection The invention relates to a formula and a preparation process of aztreonam for injection. The preparation process comprises the following steps of: preparing; removing pyrogen; degerming, namely, filtering a prepared liquid medicament with a 0.22 mu m grade filter membrane within 8 hours for degerming; filling, namely, filling the degermed liquid medicament into a small bottle within 8 hours; performing freeze drying, namely, transferring the small bottle filled with the liquid medicament onto a shelf board of a freeze dryer, pre-freezing at the temperature of 40 DEG C below zero for 2 to 3 hours, setting the temperature of the shelf board to be between 0 and 8 DEG C at a primary drying stage, setting the vacuum degree to be between 5 and 15 Pa and drying for about 19 hours until the temperature of the product is close to the set temperature; and setting the temperature of the shelf board to be between 30 and 40 DEG C at a secondary drying stage, setting the vacuum degree to be between5 and 15 Pa, drying for 3 to 5 hours until the temperature of the product is more than 25 DEG C, restoring the pressure of a freeze drying box to atmospheric pressure, compressing a bottle plug and removing the small bottle from the freeze drier. The preparation process has the advantages of short period, low energy consumption and the like.
CN1861610A Synthesizing of Demethylcantharidin-neodymium A metallic organic compound 'norcantharidin-Nd' with high effect to prevent and treat liver cancer is prepared from dehydronorcantharidin through addition reaction and complex reaction.
EP1126869B1 Methods for regulating angiogenesis and vascular integrity using the trk receptor ligands bdnf, nt-3 and nt-4 The present invention relates to methods of inducing or inhibiting the angiogenic process and promoting vessel growth or stabilization in an organ by modulating the trk receptor pathway. The present invention also relates to a method for treating a pathological disorder in a patient which includes administering a trk receptor ligand or an inhibitor or expression or activity of a trk receptor ligand. The present invention also relates to a method of screening for a modulator of angiogenesis, vessel growth, or vessel stabilization. Another aspect of the present invention is a method of diagnosing or monitoring a pathological disorder in a patient which includes determining the presence or amount of a trk receptor ligand or activation of a trk receptor ligand in a biological sample.
EP1274430B1 Cabergoline for the treatment of fibromyalgia and chronic fatigue syndrome The present invention provides for the use of a heterocyclic amine-type compound, a substituted phenylazacycloalkane-type compound, or a cabergoline-type compound to prepare a medicament for the treatment of symptoms of fibromyalgia syndrome, or chronic fatigue syndrome.
CN101757625A Nasal pharmaceutical composition of cyclodextrin inclusion cortin and H1 receptor antagonist The invention relates to a nasal pharmaceutical composition of cyclodextrin inclusion cortin and an H1 receptor antagonist, comprising the cortin and the H1 receptor antagonist which are used as active components. The invention is characterized in that the cortin and/or the H1 receptor antagonist which are used as the active components in the pharmaceutical composition are treated by inclusion of cyclodextrin and/or derivatives thereof. The pharmaceutical composition is used for curing allergic rhinitis of people or mammals.
EP1265606B9 Cell adhesion inhibitors A cell adhesion inhibitor of the general formula: R?3-L-L'-R1¿ is disclosed. An inhibitor of the present invention interacts with VLA-4 molecules and inhibits VLA-4 dependent cell adhesion. Also disclosed are methods for preparing and using such a cell adhesion inhibitor, as well as pharmaceutical compositions containing the same.
US20120141376 Prostate specific transcripts and the use thereof for prostate cancer therapeutics and diagnostics Genes that are up regulated in human prostate tumor tissues and the corresponding proteins are identified. These genes and the corresponding antigens are suitable targets for the treatment, diagnosis or prophylaxis of prostate cancer.
EP1177190B1 USE OF SELECTIVE ANTAGONISTS OF THE ALPHA 1b-ADRENERGIC RECEPTOR FOR IMPROVEMENT OF SEXUAL DYSFUNCTION Compounds (I) (A=2-furyl, substituted 2-furyl, 2-tetrahydrofuryl, substituted alkoxy or substituted phenoxyalkyl; B=B1, B2 or B3, but if B=B1 then A=substituted phenoxyalkyl) and their enantiomers, diastereoisomers and pharmaceutically acceptable salts are useful for the preparation of a medicament for the treatment of sexual dysfunction in males and females. Compounds II (I:B=B3, A ≠ 2-furyl) are novel and are claimed per se. Pharmaceutical compositions containing compounds II are also claimed, as are pharmaceutical compositions containing compounds I and one or more of a prostaglandin, a direct vasodilator and a 5 cGMP phosphodiesterase inhibitor (e.g. sildenafil). Compounds which bind to mammalian α1b adrenergic receptors with an affinity of at least about 10-8 M and which bind to mammalian α¿1b? adrenergic receptors with an affinity at least 10-fold higher than the affinity with which the compound binds to mammalian α1a or α1d α1L adrenergic receptors are also useful for the preparation of a medicament for the treatment of sexual dysfunction in males and females. A method of identifying such compounds is also disclosed and claimed.
US20070004761 Pyrazolo [3,4-d] pyrimidine derivatives and their use in the treatment of h.pylori infection This invention relates to novel compounds having the structural diagram (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of H. pylori infection.
US20090170900 Dosing regimen for weight loss Disclosed are dosing regimens and methods for the treatment of obesity, overweight and/or overeating in mammals comprising administering to the mammal a pharmaceutically effective amount of a CB1 receptor antagonist as a unit dosage according to a continuous schedule having a dosing interval selected from the group consisting of once-weekly dosing, twice-weekly dosing, thrice-weekly dosing, biweekly and bimonthly.
US20080171072 Ocular inserts containing apomorphine A gelatin-based insert was designed to deliver apomorphine by the ocular route. A clinical trial showed the product to have an efficacy similar to intravenously-administered apomorphine with a better safety profile in terms of adverse effects.
WO2011110087A1 Combined use of ribonuclease and artemisinsin A kit is disclosed. It comprises an agent comprising an artemisinin or an artemisinin derivative; an agent comprising a ribonuclease; and a description.
WO2004096194A3 Prevention of hiv-1 infection by inhibition of rho-mediated reorganization and/or content alteration of cell membrane raft domains The invention generally relates to a method of preventing or slowing down a retroviral infection through the use of agents which prevent the aggregation of retroviral receptors that are associated with the raft domains of the cell membranes. More specifically, the invention relates to the prevention or treatment of a HIV-1 infection through the use of agents which inhibit the activation of Rho-A, by acting on GTPase activity or on protein isoprenylation. The invention also relates to a method of preventing or slowing down a HIV-1 infection by moving the receptors for cytokines of the raft domains of the cell membranes.
EP2393814A1 Pyrrolopyrimidinyl axl kinase inhibitors Compounds represented by Formula (I): are useful in treating diseases, such as cancer, that are mediated and/or associated (at least in part) with AxI kinase. The compounds can be formulated as pharmaceutically acceptable compositions for administration to a subject in need thereof.
WO2005030193A1 4-(phenyl-ethylideneaminoxy-propoxy) -phenyl-acetic acid derivatives and related compounds as pai-1 inhibitors for the treatment of impairment of the fibrinolytic system and of thrombosis The present invention relates to substituted aryl oximes of formula (I) or a pharmaceutically acceptable salt or ester form thereof wherein R1 is a direct bond to A, C1-C4 alkylene, or -O-C1-C4 alkylene; R2 and R3 are , independently hydrogen, halogen, C1-C4 alkyl, C1-C3 perfluoroalkyl, -O-C1-C3 perfluoroalkyl, C1-C3 alkoxy, -OH, -NH2, -NO2, -O(CH2)p-aryl, -O(CH2)p-heteroaryl, aryl, heteroaryl, -NH(CH2)p-aryl, -NH(CH2)p-heteroaryl, -NH(CO)-aryl, -NH(CO)-heteroaryl, -O(CO)-aryl, -O(CO)-heteroaryl, -NH(CO)-CH=CH-aryl, or -NH(CO)-CH=CH-heteroaryl; p is an integer from 0-6; R4 is hydrogen, C1-C8 alkyl, or C3-C6 cycloalkyl; A is COOH or an acid mimic; X is C1-C8 alkylene, C3-C6 cycloalkylene, -(CH2)mO-, or -(CH2)mNH-; m is an integer from 1-6; R5 and R6 are, independently, hydrogen, halogen, C1-C6 alkyl, C1-C6 perfluoroalkyl, -O-C1-C6 perfluoroalkyl, C1-C6 alkoxy, -OH, -NH2, -NO2, -O(CH2)n-aryl, O(CH2)n-heteroaryl, aryl, or heteroaryl; and is an integer from 0-6, wherein C1-C4 alkaline, -O-C1-C4 alkaline, alkyl, aryl and heteroaryl are each optionally substituted by one or more substituents. The present compounds are PAI-1 inhibitors for the treatment e.g of impairment of the fibrinolytic system, thrombosis or cardiovascular diseases.
US7179476 Medical composition for external use for dermatosis The object of the present invention is to provide a dermal composition for external use which keeps skin healthy and demonstrates a sufficient effect in treating skin diseases. The present invention relates to a dermal composition for external use, which comprises sodium cromoglycate and a monoester of polyvalent alcohol and salicylic acid contained in a base.
CN101053567A Acetylcholinesterase inhibitor, its preparation method and application The invention provides an acetylcholinesterase inhibitor using anisaldehyde-huperzine aldimine compound or vanillin-huperzine aldimine compound or trans-cinnamaldehyde-huperzine aldimine compound as the active compound, preparation method thereof and application in preparing acetylcholinesterase inhibitor, medicine for treating Alzhemed and memory and recognition reduction diseases of the aged people.
CN101601742A Preparation method of ointment for curing infantile tinea favosa The invention discloses a preparation method of an ointment for curing infantile tinea favosa in the technical field. The infantile tinea favosa can be cured within 2 days by using the method. The method is realized by adopting the following technical scheme that: goldthread root is processed into 200 meshes of fine powder, and then mercurous chloride and borneol are uniformly ground and put in a refrigerating chamber to be refrigerated for 36 hours and then blended into ointment with rhizoma optidis powder and sesame oil after being taken out to obtain the finished medical ointment.
EP1117356B1 Apparatus for improved administration of fentanyl and sufentanil Methods and apparatus for improving administration of analgesics through the use of heat. The present invention relates to the use of heat in conjunction with specially designed transdermal analgesic delivery systems and conventional commercial transdermal analgesic delivery systems to alter, mainly increase, the analgesic release rate from the transdermal analgesic delivery systems or the depot sites to accommodate certain clinical needs.
EP2203426A1 Benzenesulfonamide compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor The invention relates to compounds of the formula R1 is selected from the group consisting of hydrogen, linear C1-C3 alkyl and fluorinated linear C1-C3 alkyl; R2 is hydrogen or methyl; R3 is selected from the group consisting of hydrogen, halogen, C1-C2-alkyl, fluorinated C1-C2-alkyl, C1-C2-alkoxy and fluorinated C1-C2-alkoxy, R4 is C1-C2-alkyl or fluorinated C1-C2-alkyl; n is 0, 1 or 2, and the physiologically tolerated salts of these compounds and the N-oxides thereof. The invention also relates to a pharmaceutical composition that comprises at least one compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.
EP2457907A1 Flavagline derivatives as neuroprotective agents The present invention discloses new flavagline derivatives (I) and the use of these compounds as neuroprotective and/or cardioprotective and/or antitumoral agents. In particular, the present invention discloses the use of these flavagline derivatives to prevent or limit the neurotoxicity of an antineoplastic agent. The use of these new compounds to prevent or treat a neurodegenerative disease of the nervous system, in particular Parkinson's disease, is also disclosed.
CN102919269A Povidone-iodine disinfectant and preparation method thereof The invention discloses a povidone-iodine disinfectant and a preparation method thereof. The povidone-iodine disinfectant comprises povidone-iodine (PVP-I), potassium iodate and potassium iodide. Critic acid and sodium hydroxide are used for adjusting the pH of a solution. The povidone-iodine solution contains potassium iodate and potassium iodide, and under an acid environment, a reaction of IO3<->+5I<->+H<+>=3I2+3H2O exists in the solution. Effective iodine concentration in the solution is increased, active iodine is promoted to be released slowly, and disinfecting time of the povidone-iodine disinfectant is prolonged.
EP2563785A1 Compounds as agonists of s1p1 receptors Compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by S1P1 receptors.
US20090318474 Pyridine and pyrimidine derivatives as mglur 2 antagonists The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.
CN1973823A Anticancer composition containing Synergist The anticancer composition containing synergist is one kind of slow releasing injection and slow releasing implant. The slow releasing injection consists of slow released microsphere comprising effective anticancer component and slow releasing supplementary material, and special solvent containing suspending agent. The suspending agent is selected from sodium carboxymethyl cellulose, etc, and has viscosity of 100cp-3000cp. The slow releasing implant consists of effective anticancer component and slow releasing supplementary material. The slow releasing supplementary material is selected from polylactic acid, polifeprosan, etc. The effective anticancer component is composition of anticancer medicine phosphoinositide-3-kinase inhibitor, pyridine analog, etc and the synergist rapamycin. The slow releasing injection and the slow releasing implant may be used alone to inhibit the growth of tumor or in conjunction with chemotherapy to raise the curative effect.
WO2013087042A1 Medical composition for preventing or treating amyloid β peptide related diseases or conditions A medical composition containing acteoside and isoacteoside is capable of inhibiting the generation, accumulation or concentration of amyloid β peptide, and can be therefore used to prevent or treat amyloid β peptide related diseases or conditions. The ratio of the weight of the isoacteoside to that of the acteoside ranges from 4:1 to 1:4.
CN102038796A Externally applied medicament for treating burns and preparation method thereof The invention relates to an externally applied medicament for treating burns and a preparation method thereof. The externally applied medicament is characterized by comprising the following selected raw material medicines in part by weight: 120 parts of Chinese angelica, 150 parts of raw rehmannia roots, 150 parts of lithospermum, 80 parts of coptis chinensis, 80 parts of golden cypress, 80 parts of scutellaria, 60 parts of madder, 150 parts of garden burnet and 8 parts of borneol. The combination of the selected medicinal materials has the efficacy of clearing heat, cooling blood, activating blood circulation, dispelling stasis, removing toxin, astringing wounds, purging intense heat and eliminating dampness and has the effects of removing putrefaction, promoting tissue regeneration, moisturizing wounds, relieving pain and clearing dampness. Clinic application finds that the externally applied medicament has the advantages of rapid effect taking, obvious analgesic effect, no nay toxic or side effect and no scar after curing.
CN101049357A Composition for preventing and treating osteoporosis, and preparation method A medical composition for preventing and treating osteoporosis is prepared the extract of haw and/or hawthorn leaf, and optional Ca-contained substance, VD3 and trace elements. Its preparing process is also disclosed.
CN101591321B Method for preparing 5,6,7,4'-tetrahydroxyflavone The invention provides a method for preparing a 5,6,7,4'-tetrahydroxyflavone compound, which is characterized by comprising the following steps: taking breviscapinun as a raw material, and performing heating reflux reaction between the breviscapinun and alcohol under the catalysis of acid, namely adding 200 to 500 ml of alcohol substance and 1 to 3 ml of 4 to 5 percent acid into 12 to 20 g of thebreviscapinun for the heating reflux reaction; and filtering a product, and drying to a constant weight to obtain 5,6,7,4'-tetrahydroxyflavone shown in a formula I. Experiments prove that the 5,6,7,4'-tetrahydroxyflavone shows obvious strengthening effect on acquisition, consolidation and representation of brain memory of a mice model of alzheimer disease, has obvious improving effect on learningmemory of the mice model with memory loss caused by anisodine of an M-cholinergic inhibitor, and can obviously improve the recent memory and long-term memory capacities of mice. The experiments also prove that the 5,6,7,4'-tetrahydroxyflavone has the effect of treating arthritis, and also has good treating effects on diabetes mellitus and osteoporosis.
US20100233228 Drug-Eluting Medical Device A drug-eluting medical device includes a catheter balloon completely or partially coated with paclitaxel in anhydrous crystalline form, having an immediate release and bioavailability of a therapeutically effective amount of paclitaxel at the intervention site. The balloon can be made of a polyether-polyamide block copolymer, or a polyester amide, or polyamide-12.
EP2691094A1 Alisporivir to treat hepatitis c virus infection The disclosure concerns the use of cyclophilin inhibitors in the treatment of chronic Hepatitis C virus infection.
US7125906 Indole derivatives having anti-angiogenetic activity The invention relates to the use of a compound of Formula (I), for the manufacture of a medicament to inhibit and/or reverse and/or alleviate symptoms of angiogenesis and/or any disease state associated with angiogenesis: wherein: X, p, q, R1, R2, R3, R4, and R5 are as defined in the description. The invention also related to use of compounds of Formula (I) as medicaments and also to novel compounds of Formula (I). The invention further provides pharmaceutical compositions of compounds of Formula (I) and processes for the synthesis of compounds of Formula (I).
WO2009077462A3 Chiral cycloplatinized complexes, method for the production thereof and their use in medicine and catalysts The present invention relates to a method for producing cycloplatinized platinum (II) complexes, platinum (II) complexes produced by said method, and the use thereof for treating tumor diseases and/or hemoblastosis.
CN102863436A Thiazolidinedione derivatives, preparation thereof and use thereof The invention discloses a series of derivatives (II) of which the molecules internally include 5-{4-[2-(N-methyl-N-(2-pyridyl)-azyl)-ethyoxyl]-benzyl}-2, 4-thiazolidinedione such as alcohol, ester, ether, amide, acid and the like, and a preparation method of the derivatives. The derivatives provided by the invention are a series of the derivatives (II) obtained by taking rosiglitazone sodium (I) as raw material. The derivatives have the general formula (II), wherein A is alcohol, ester, ether, amide, acid and the like which contain carbon and are formed by nitrogen atom, oxygen atom and sulphur atom. The thiazolidinedione derivatives provided by the invention have the functions for curing the diabetes mellitus and the metabolic syndrome such as blood sugar reducing, blood fat reducing and the like, thereby being wide in application in clinic.
WO2012112956A2 Compounds and methods for targeting leukemic stem cells This invention relates to high-throughput, semi-automated methods for identifying compounds that are effective in targeting leukemia stem cells, as well as compounds identified by those methods and uses thereof for treating leukemia.
WO2007097010A1 Substance fki-2342 and process for production thereof A process for producing a substance FKI-2342 comprising the steps of cultivating a microorganism belonging to the genus Aspergillus and capable of producing the substance FKI-2342 represented by the general formula (I) in a culture medium to accumulate the substance FKI-2342 in the culture and collecting the substance FKI-2342 from the culture. The substance FKI-2342 is a substance capable of inhibiting G2 checkpoint specifically and can inhibit a cancer cell specifically. Therefore, in the therapy with a DNA-damaging anti-cancer agent or a radioactive ray, the substance is expected to enahnce the effect of the therapy and reduce adverse side effects.
WO2008113320A1 Lejimalid analoga and uses thereof The invention relates to Ijemalide having the following formula (I) in which a, b, c, d, e, f, g, h, i, j, k, I, m, n, o, p are simple or double bonds, the continuous lines representing at least one simple bond, the dotted lines representing a possible bond. A double bond can be present but it is not necessary, and provided that a continuous line is also present, or a simple bond can be present if no other line is represented; m = 0 - 20 and n1 - n18 = 1, 2. The bonds can be used as chemotherapeutic agents for treating cancer.
US20090181904 Method for regulating nutrient absorption with ginsenosides The present application relates to a method of regulating nutrient absorption in a subject in need thereof with an isolated ginsenoside compound.
CN102846655A Formulation and preparation method of antibacterial spray The invention discloses a formulation and a preparation method of an antibacterial spray with antibacterial, hemostasis and promotion of wound healing effects. The spray contains water which is used as a solvent, and chitosan, glycerol, polyhexamethylene guanidine and vitamin E which are used as main effective components. The antibacterial spray has obvious activity inhibition on growth of multiple types of pathogenic bacteria, the killing rate of the antibacterial spray on staphylococcus aureus, escherichia coli and candida albicans can reach 99%, and the antibacterial spray does not stimulate skins and mucosa, is suitable for treating skin and mucosa wound surface infection, and can be used for promoting the wound healing.
EP2651888A1 New compounds for the treatment of neurodegenerative diseases This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.
US20080234349 PPAR active compounds Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ.
CN103539709A N-(-1-hydro-indenyl-1-yl)sulfonamide compound and its preparation method and use The invention provides a compound. The compound is an N-(-1-hydro-indenyl-1-yl)sulfonamide compound shown in the formula I, or its enantiomer, diastereoisomer, raceme, pharmaceutically acceptable salt, crystalline hydrate or solvate. The N-(-1-hydro-indenyl-1-yl)sulfonamide compound can be used for preparation of drugs for treating or preventing thromboxane receptor-related diseases or for treating or preventing thrombosis and/or hypertension.
US20090215681 Methods of Diagnosis and Treatment of Metabolic Disorders The invention features diagnostic methods for metabolic disorders (e.g., diabetes and obesity), methods for screening for compounds useful in the treatment of metabolic disorders, and methods for treatment of metabolic disorders that involve sirtuin2 or sirtuin3 nucleic acids or proteins or their agonists or antagonists.
WO2011120339A1 Microemulsion formulation containing arctigenin A microemulsion formulation contains arctigenin and microemulsion carriers, said microemulsion carriers comprise oil phase and emulsifier, and the microemulsion has an average particle size of 10-90 nm.
US20090060990 Nsaid formulations, based on highly adaptable aggregates, for improved transport through barriers and topical drug delivery The invention describes novel formulations of nonsteroidal anti-inflammatory drugs (NSAIDS) based on complex aggregates with at least three amphipatic components suspended in a suitable, e.g. pharmaceutically acceptable, polar liquid medium. A suitably ionised NSAID is one of the two, amongst said three, components that tends to destabilise lipid membranes, the other system component with such activity being typically a surfactant. In contrast, the remaining amongst said at least three amphipatic components typically forms a stable lipid membrane on it's own. An essential characteristics of the resulting, relatively large, aggregates is an improved ability to penetrate pores, in a semi-permeable barrier, at least 30%, and often much smaller than the average diameter of the complex aggregate. This enables said aggregates to mediate NSAID transport through semi-permeable barriers including mammalian skin. As a result of the skin penetration by NSAID loaded large aggregates, the drug delivered transcutaneously with such carriers gets deeper into the tissue than the corresponding NSAID from a solution on the skin surface. This is believed to be due to the special ability of suitable large carriers to bypass the local sink of blood capillaries at the epidermal-dermal junction in the skin. The carrier-mediated delivery of locally applied NSAIDs thus allows therapy of deep tissues under the drug administration site, which is medically highly desirable.
WO2013170774A1 Acetylene derivative having antineoplastic activity The present invention relates to an aromatic ring disubstituted acetylene derivative of formula I, a pharmaceutical composition comprising the compound, and a use of the compound and of the pharmaceutical composition in the treatment and/or prevention of tumors, where A, B, T, M, Ra, Rb, Rt, m, n, and p are as defined in the present document.
CN103655535A Medical application of diacerein in treating diabetes and diabetic nephropathy The invention discloses a rhein derivative, in particular relates to a medical application of diacerein as an SGLT-2 (sodium-glucose co-transporter 2) inhibitor in treating diabetes, and further discloses the medical application of diacerein in treating diabetic nephropathy.
EP1441739B1 Use of (11beta, 17beta)-11-(1,3-benzodioxol-5-yl)-17-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one in the treatment of major depressive disorder The present invention relates to the use of the glucocorticoid receptor antagonist (11beta,17beta)-11-(1,3-benzodioxol-5-yl)-17-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one (Org 34517) for the preparation of a medicament for the treatment of depression as well as to pharmaceutical preparations of Org 34517 for said use.
EP2725016A1 Heterocyclic carboxylic acid ester derivative The present invention provides a blood glucose elevation inhibitor having a serine protease inhibitory action, which is a novel therapeutic or prophylactic agent for obesity. A compound represented by the following formula (I) wherein each symbol is as described in the specification, or a pharmaceutically acceptable salt thereof.
CN102302462A Gemcitabine hydrochloride lyophilized preparation The present invention discloses a gemcitabine hydrochloride lyophilized preparation. The lyophilized preparation comprises, by weight, 20-70 parts of gemcitabine hydrochloride, 15-60 parts of a lyoprotectant and 0.005-0.5 parts of an antioxidant. Compared to the prior art, with the gemcitabine hydrochloride lyophilized preparation provided by the present invention, the problem of the stability ofthe gemcitabine hydrochloride is solved; the product quality is ensured; the risk of drug using is reduced; the preparation process is simple, the cost is low; and the preparation is suitable for theindustrial production, and has practical value.
EP2603211A1 Composition for treating hyperlipidemia It is disclosed a combinatory preparation for treating hyperlipidemia and/or hypercholesterolemia comprising pyrrozilidine alkaloids and preferably whole, parts or and/or a leeching or extract of a plant from the family Asteraceae and preferably Gynura divaricata DC in combination with one or more other lipid and/or cholesterol-reducing substances. The combinatory preparation displays an improved effect as compared to other synthetic cholesterol-reducing medications.
US6919438 Comprises viral expression vector coding envelope protein domains for use as gene therapeutic tool in the treatment of autoimmune diseases The invention concerns a novel nucleic sequence and deduced protein sequence family with whole or partial human endogenous retroviral motifs. The invention also concerns the detection and/or the use of said nucleic sequences and said corresponding protein sequences or fragments of said sequences, for diagnostic, prophylactic and therapeutic uses, in particular for neuropathological conditions with autoimmune constituent such as multiple sclerosis. Said purified nucleic acid sequences comprise all or part of a sequence coding for a human endogenous retroviral sequence having at least eny-type retroviral motifs, corresponding to the sequence SEQ ID NO:1 or to a sequence having a homology level with said sequence SEQ ID NO:1 not less than 80% of more than 190 nucleotides or not less than 70% on more than 600 nucleotides for env-type domains. The invention further concerns the use of the flanking or adjacent sequence of said sequences and controlled by the latter, as diagnostic reagents.
CN102895206A Rhizoma bletillae polysaccharide gastric-floating tablet and preparation method and application thereof The invention discloses a preparation method for a rhizoma bletillae polysaccharide gastric-floating tablet and an application of the rhizoma bletillae polysaccharide gastric-floating tablet and belongs to the technical field of new uses of drugs. The invention relates to a new formulation of rhizoma bletillae polysaccharide, and the new formulation of the rhizoma bletillae polysaccharide is used for treating a gastric ulcer. The gastric-floating tablet is prepared through matching the rhizoma bletillae polysaccharide, xanthan gum and glyceryl behenate by the preparation method disclosed by the invention. The rhizoma bletillae polysaccharide gastric-floating tablet has the characteristics that the preparation method is simple, and a treatment effect on a peptic ulcer is good.
US20080255075 Treatment or inhibition of a steroid hormone dependent disorder; reducing spermatogenesis or male virility; 17 beta -hydroxysteroid dehydrogenase (17 beta-HSD) inhibitors; compounds such as 3-(benzylamino)-15alpha-(4-morpholin-4-yl-4-oxobutyl)estra-1(10),2,4-trien-17-one Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17β-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.
US7348359 Retinoid X receptor modulators The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.
EP1567146B1 Iontophoretic delivery of rotigotine for the treatment of parkinson's disease By using a composition comprising rotigotine and at least one chloride salt in a concentration of 1 to 140 mmol/l, the composition having a pH of 4 to 6.5 in a iontophoretic device for the treatment of Parkinson's disease, it became possible to obtain a rotigotine flux across the human stratum corneum which was higher than the one previously obtained with conventional passive diffusion systems.
US20050220845 Foods and drinks having health benefits and method for adding health benefits to foods and drinks Problem to be solved: To provide foods and drinks having health benefits or enriched with health benefits and a method for adding strong health benefits to foods in a wide range. Solution: The present invention provides foods and drinks, having health benefits, or enriched with health benefits, comprising as an active ingredient a hydrogenated, hardly digestible dextrin obtainable by digesting pyrodextrin with an enzyme and then hydrogenating the digested dextrin. The present invention also provides a method for adding health benefits to foods and drinks or for increasing the health benefits in foods and drinks, which comprises the steps of adding at least 3 g/meal or 3 g/day, in terms of hardly digestible components, of the hydrogenated, hardly digestible dextrin to foods or drinks to foods or drinks, or replacing at least a part of the foods or drinks with the hydrogenated, hardly digestible dextrin.
WO2011009484A1 Arylpyrazoles and arylisoxazoles and their use as pkd modulators The present invention provides novel organic compounds of formula (I) or (Ia): which may be inhibitors of a selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example PKD-1/2/3, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. The selectivity of which would depend on the structural variation thereof, and for treatment of a disorder or disease mediated by those selected AGC or calmodulin family kinases. These organic compounds can be used to treat various PKD associated states such as heart failure, colorectal cancer, regulation of cell growth, autoimmune disorders, or hyperproliferative skin disorders.
US20100158843 Novel 3-phenylpropanoic compound activators of receptors of ppar type and pharmaceutical/cosmetic compositions comprised thereof Novel 3-phenylpropanoic acid compounds have the general formula (I) below: and are formulated into pharmaceutical compositions for administration in human or veterinary medicine (in dermatology, and also in the field of cardiovascular diseases, immune diseases and/or lipid metabolism-related diseases), or, alternatively, into cosmetic compositions.
CN101547902B pyridine derivatives for treatment of metabolic disorders related with insulin resistance and hyperglycemia The present invention provides novel compounds represented by the general formula (I): wherein Ar is a quinoline or isoquinoline moiety which is substituted or unsubstituted; B is -O. -S-. or -NH-: R<1> is hydrogen or S(O)2R<4>: R<2> is S(O)2R<4>. C(O)OR<5>. or C(O)(CH2)n-C(O)OR<6>: R<3> is halogen, cyano, C(O)OR<7>. or C(O)NR<8>R<9>: R<4> is aryl: R<5> is (C1-C6)alkyl or aryl: R<6> is hydrogen. (C1-C4)alkyl. or aryl: R<7> is hydrogen or (C1-C4)alkyl: R<8> and R<9> are independently hydrogen or (C1-C6)alkyl; n is an integer from 1-3: and a pharmaceutically acceptable salt or solvate thereof. their pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The invention also relates to a process for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them.
US7879848 Dipeptidyl Peptidase-IV inhibiting compounds, method of preparing the same, and pharmaceutical compositions containing the same as an active agent Novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV(DPP-IV) include those of the following formula (1) or pharmaceutically acceptable salt thereof: wherein A is a substituted or unsubstituted 1,4,5,7-tetrahydro-pyrazolo[3,4-c]pyridine, 5,6 -dihydro-8H-[1,2,4]triazolo[4,3-a]pyrazine, 4,5-dihydro-7H-isooxazolo[3,4-c]pyridine, 3,4 -dihydroisoquinoline, 5,8-dihydropyrido[3,4-d]pyrimidine, or 6,7 -dihydro[1,3]thiazolo[4,5,c]pyridine, and B is a substituted or unsubstituted piperidin-2-one, morpholin-3-one, oxazolidin-2-one, pyrrolidin-2-one, or 1,5-dihydro-pyrrol-2-one. Methods of preparing the novel inhibitory compounds of formula (1) and pharmaceutical compositions containing the same as an active agent are disclosed.
CN101502513A Rifaximin sustained-release preparation composition and method for preparing the same The invention discloses a rifaximin sustained-release preparation combination and a preparation method thereof. The rifaximin sustained-release preparation combination is mainly prepared from rifaximin bulk drugs, sustained-release materials and other appropriate auxiliary materials. The rifaximin sustained-release preparation provided by the invention can deaccelerate the release rate of the main drugs, reduce the frequency of administration and improve the patient compliance. The invention provides a novel form of drug having better patient compliance and having the advantages of high quality controllability and stability of the preparation process.
EP2314578A1 Cinchonidine salt of (4S,5S)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid, useful as intermediate in the preparation of cannabinoid CB1 neutral antagonists The present invention relates to a cinchonidine salt of (4S,5S)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid. This cinchonidine salt is prepared by enantiomeric resolution of a compound of formula (I) comprising: the reaction of compound of formula (I) with cinchonidine in a suitable solvent, thereby resulting in the cinchonidine salt of the enantiomer (4S,5S) of formula (II); and optionally isolating said salt. The cinchonidine salt according to formula (II) is a useful intermediate in the preparation of a cannabinoid CB1 neutral antagonist.
DE102009049332A1 Medicinal substance, useful e.g. for treating hemorrhoidal disease, comprises lactulose, which is used for supplying nutrients to the mucous membrane of the colon, pH adjustment and stabilizing the physiological intestinal flora rectally Medicinal substance comprises lactulose, which is used for supplying nutrients to the mucous membrane of the colon, pH adjustment and stabilizing the physiological intestinal flora rectally. - ACTIVITY : Vasotropic; Gastrointestinal-Gen. No biological data given. - MECHANISM OF ACTION : None given.
WO2007075605A3 Use of beta-hydroxy-beta-methylbutyrate to modulate the imbalance in type and type 2 cytokine production Disclosed are methods of treating an individual having a condition characterized by an imbalance in type (1) and type (2) cytokine production, wherein the method comprises administering to the individual an amount of β -hydroxy- β -me thylbutyrate (HMB) effective to modulate or otherwise cause an increase in the ratio of type (1) to type (2) cytokines, including an increase in the ratio of type (1) to type (2) cytokines without a corresponding increase in type (2) cytokine levels. Also disclosed are methods of using HMB to treat asthma, allergies and cancer. The methods of the present invention are based upon the discovery that HMB modulates cytokine production, most typically by increasing type (1) cytokines without a corresponding increase in type (2) cytokines.
WO2013173330A1 Compositions comprising zoledronic acid or related compounds for relieving inflammatory pain and related conditions Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions. Although an oral dosage form with enhanced bioavailability with respect to the bisphosphonate compound can be used, the treatment can also be effective using an oral dosage form that includes a bisphosphonate compound, such as zoledronic acid, wherein the bioavailability of the bisphosphonate is unenhanced, or is substantially unenhanced.
US20110262364 Fluorescent Particles Comprising Nanoscale ZnO Layer and Exhibiting Cell-Specific Toxicity A core-shell nanoparticle having a core that includes a fluorophore and a first oxide of a first metal and a shell that includes a second oxide of a second metal such that the first oxide and the second oxide are different. Also disclosed are methods relating to the core-shell nanoparticle.
US20100166661 siRNA COMPOSITIONS AND METHODS FOR POTENTLY INHIBITING VIRAL INFECTION No antiviral regimen has been consistently successful in treating H5N1 virus infection. We demonstrate that a group of highly effective siRNAs targeting different H5N1 viral genes shares a unique motif, GGAGU/ACUCC. We further demonstrate that the effectiveness of siRNAs containing this motif is not sequence specific. The results suggested that the structure of the unique motif is critical in determining the potency of siRNA-mediated protective effects against viral infection and this potent in vivo protection is associated with early productions of β-defensin and IL-6 induced by the motif. Provided are methods and prophylactic and therapeutic agents useful against other viral infections in addition to the H5N1 influenza virus.
EP1485084B9 Use of an l-ascorbic acid salt to prepare a pharmaceutical composition for ophthalmic topical use capable of improving the level of l-ascorbic acid in the eye Use of a salt of L-ascorbic acid with a pharmaceutically acceptable organic base to prepare a pharmaceutical composition, for ophthalmic topical use, capable of improving the level of L-ascorbic acid in a human eye.
EP1808169A2 Polyhydroxylated aromatic compounds for the treatment of amyloidosis and alpha-synuclein fibril diseases Polyhydroxylated aromatic compounds, and compositions containing them, are useful for the treatment of amyloidosis, especially Alzheimer's disease, and for the treatment of diseases characterized by α-synuclein fibril formation, especially Lewy body disease and Parkinson's disease.
EP1156821B1 Treatment of infertility In an in vitro fertilisation method, a woman is treated with a hypothalamic hormone and/or a pituitary hormone or an agonist or antagonist thereof or an active derivative thereof for a short period of time and, thereafter, using in vitro oocyte maturation egg or eggs are retrieved from the woman and are maturated using a meiosis activating compound.
US20110002989 Methods, dosage forms and kits for administering ziprasidone without food The present invention provides methods, dosage forms and kits for treating with an effective amount of ziprasidone a CNS disorder in a human when the human is in a fasted state. In one embodiment, the invention relates to a method for treating a CNS disorder in a human, which method comprises administering to the human in a fasted state, a solid oral dosage form comprising an amount of ziprasidone effective to treat said CNS disorder, wherein the area under the serum concentration versus time curve (AUC0-inf) of the ziprasidone in the human subsequent to said administering is from 70% to 140% of the mean area under the ziprasidone serum concentration versus time curve (AUC0-inf) resulting from administration of a control ziprasidone immediate release oral capsule containing the same amount of ziprasidone to a cohort of humans in a fed state.
CA2857400A1 Method for treating breast cancer Breast cancer cells lacking ER protein expression, PgR protein expression and/or showing absence of HER2 protein over-expression (i.e., triple-negative breast cancer cells, basal-like) can be efficiently targeted with an anti-KAAG1 antibody and killed upon delivery of a therapeutic moiety. Antibodies and antigen binding fragments that specifically binds to KAAG1 may thus be used for the, detection and therapeutic treatment of breast cancer cells that are negative for at least one of these markers. The use of antibody conjugates in the treatment of triple-negative breast cancer and/or basal-like breast cancer is disclosed herein.
US20120015020 Biodegradable drug or other active delivery system A nonwoven fabric has been developed as a delivery system for drugs or other actives which includes biodegradable and biocompatible fibers with plant virus nanoparticles. The plant virus nanoparticles are pre-loaded with one or more actives.
US6992188 Nitrogen compounds such as 2,5,6-trimethyl-7-(1-propylbutyl)-4-(2,4,6-trimethylphenoxy)-7H-pyrrolo[2,3-d]pyrimidine, used as Corticotropin-releasing factor (CRF) antagonists Corticotropin-releasing factor (CRF) antagonists having the formula wherein the dashed lines, A, B, D E, F, Z, G, R3, and R5 having the definitions set forth in the specification pharmaceutical compositions containing them.
CN101589047A Cathepsin proteases inhibitors The invention provides compounds (I) and pharmaceutical compositions thereof, and more particularly, bicyclic carbamates, which are useful as cathepsin inhibitors, and methods for using such compounds or pharmaceutically acceptable salts thereof, wherein X is 0 or S; R is OR, halo, (CR2)nR, nitro, cyano, amino, aniido, sulfonamide, or an optionally substituted C1-6 alkyl, C2-6 alkenyl, or C3-6 alkynyl;R is H, (CR)nR, or an optionally substituted C1-6alkyl, C2-6 alkenyl or C3-6 alkynyl; R is an optionally substituted aryl, heteroaryl, carbocyciic ring or heterocyclic ring; m is 1-3; and n is 0-4.
US7803354 Cosmetic and/or dermatological use of a composition comprising at least one oxidation-sensitive hydrophilic active principle stabilized by at least one maleic anhydride copolymer A method for depigmenting and/or lightening the skin and/or hair, including body hair, including applying a composition including at least one oxidation-sensitive hydrophilic active principle chosen from ascorbic acid and its derivatives and at least one maleic anhydride copolymer, comprising one or more maleic anhydride comonomers and one or more comonomers chosen from vinyl acetate, vinyl alcohol, vinylpyrrolidone, olefins comprising from 2 to 20 carbon atoms, and styrene, in a physiologically acceptable medium comprising an aqueous phase, to the skin and/or hair.
EP1343781B1 Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases The present invention provides compounds of formula I:wherein G is a small group selected from hydrogen or C1-3 alkyl, Q is pyridine or pyrimidine, and R1 - R3 are as defined in the specification. These compounds are selective JNK inhibitors showing good activity against the three isoforms of JNK (JNK1, JNK2 and JNK3) and relatively low activity against p38 kinase. The compounds are therefore usefull for treating JNK-mediated diseases, especially neurodegenerative diseases in which all three JNK isoforms are implicated.
CN102379864A Compound salvianic acid injection for treating cerebral vascular thrombosis diseases and preparation process thereof The invention aims to provide a compound salvianic acid injection which uses salvianic acid and paeonol as main components with high efficiency, advanced dosage form and stable preparation, as well as a preparation process thereof, and belongs to the field of biological pharmacy. The method comprises the following steps: extracting salvianic acid from salvia, and extracting paeonol from peony bark and enamelling with 2-hydroxypropyl-beta-cyclodextrin to prepare paeonol- hydroxypropyl-beta-cyclodextrin clathrate compound; weighting and mixing the salvianic acid, the paeonol clathrate compound and an excipient according to marked weights in the prescription, dissolving with injection water, filtering, and regulating the pH of the filtrate to be between 6.8 and 7.2; sterilizing and filtering, and diluting with aseptic injection water to the total designing solution; and packaging in a brown glass tube vial, and lyophilizing. The injection has the effects of activating blood circulation to remove stasis, and dredging collaterals and relieving pain, and is suitable for patients with cerebral vascular thrombosis diseases, such as coronary heart disease, angina pectoris, cerebral thrombosis, cerebral infarction and the like. The injection for adults is used for intramuscular injection or intravenous drip, and is dosed 1 to 5 vials one time, 1 to 2 times per day or as professionally prescribed.
US20080248099 using insulin for making medicine to treat Alzheimer's disease, brain atrophy associated with diabetes, Parkinson's disease, Huntington's Disease, senile dementia, multiple sclerosis, dementia associated with Acquired Immunodeficiency Syndrome (AIDS), Pick's Disease, stroke, trauma; tolbutamide The present invention provides a use of an insulin for the manufacture of a medicament for treating or preventing diseases or disorders of adult brain. Also provided is a method for treating or preventing diseases or disorders of adult brain by administering an effective amount of an insulin to the brain. The diseases or disorders of adult brain are associated with tissue shrinkage or atrophy. The amount of the insulin administered is preferably from 0.001 Units per kg body weight per day up to 10 Units per kg body weight per day.
US7670625 Pharmaceutical composition containing an active ingredient and a micronised carrier/diluent The invention relates to a stable pharmaceutical composition useful in the treatment of respiratory disorders such as asthma, rhinitis and chronic obstructive pulmonary disease (COPD) and a novel micronisation process for manufacturing a stable formulation for formoterol or its enantiomers and a carrier/diluent comprising a carbohydrate such as lactose.
CN102406898B Drug for treating psoriasis vulgaris, and preparation method thereof The present invention discloses a drug for treating psoriasis vulgaris, and a preparation method thereof. The raw materials of the drug comprise, by weight, 350-450 parts of twelfth lunar month lard, 20-30 parts of sulfur, 18-22 parts of wenchow turmeric root tuber, 18-22 parts of scorpion, and 0.26-0.34 parts of musk. The preparation method comprises: a, storing the twelfth lunar month lard for three years to provide a spare use; b, taking various raw materials according to the weight part ratio; c, grinding the sulfur, the wenchow turmeric root tuber, the scorpion and the musk into fine powder, screening the powder with a fine sieve having 80-100 meshes, mixing the resulting twelfth lunar month lard from the step a and the resulting powder, and uniformly pounding to obtain the drug for treating the psoriasis vulgaris. According to the present invention, the twelfth lunar month lard is adopted as the envoy drug, the drug can deeply penetrate skin and grain, such that the drug can directly act on the local, and penetrate the tissues so as to improve the microenvironment, promote function recovery and easily provide the effects; the twelfth lunar month lard stored for three years is adopted as the medicinal usher, such that the skin can not be damaged, and the therapeutic effect is good.
US7144915 Crystalline forms of [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt (2:1) Novel crystalline forms of [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form V, Form VI, Form VII, Form VIII, Form IX, Form X, Form XI, Form XII, Form XIII, Form XIV, Form XV, Form XVI, Form XVII, Form XVIII, and Form XIX are characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, and Alzheimer's disease.
US8623609 Proteins expressed by Mycobacterium tuberculosis and not by BCG and their use as diagnostic reagents The present invention is directed to proteins expressed by Mycobacterium tuberculosis and not by BCG and their use as diagnostic reagents.
US20110118278 Carbamoyl derivatives of bicyclic carbonylamino-pyrazoles as prodrugs There are provided bicyclic carbonylamino-pyrazoles of formula (I), wherein the variables are as specified in the claims, for use as medicament, in particular for the treatment of diseases due to the malfunctioning of protein kinases (PKs), such as cancer, pharmaceutical compositions comprising such carbamoyl derivatives, and their use as prodrugs of therapeutically active agents. Method of treatment and some new bicyclic carbonylamino-pyrazoles are also object of the present invention.
WO2008083543A1 Nitrogen-containing heterocyclic modified compounds and uses thereof A nitrogen-containing heterocyclic modified compounds and their uses in preparing the medicaments of preventing and treating the Alzheimer's disease, Parkinson's disease and other degenerative nervous system disease or type two diabetes. Studies show that the provided compounds can inhibit aggregation of Aβ, also can make the Aβ aggregated depolymerize, and will eventually hydrolysic eliminate the Aβ protein, inhibit and remove the Aβ toxicity, the said compounds has broad application prospects in the field of medicine.
US20110287065 Nanoparticulate cinacalcet compositions The invention is directed to compositions comprising stable nanoparticulate cinacalcet or a salt thereof. The composition can exhibit an improved dissolution rate, improved bioavailability, and reduced difference in absorption when administered orally under fed as compared to fasting conditions. The invention also encompasses methods of making and using such compositions.
WO2013106641A1 Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C-R7, are useful as kinase modulators, including IRAK-4 modulation.
US20070294107 Uses Of Endopeptidases In Treatment Of Disease Compounds and methods of treatment of inflammation are presented that serve to enhance MMP inhibition to block elevation of MMP activity in various disease conditions. Such treatment leads to normalization of function, blockade of the elevated levels of oxygen free radical production in the microcirculation, normalization of the elevated plasma levels of MMP 2, 9 activity, normalization of immune cell counts, and reduced apoptosis. Also included are methods of deriving value from increased sales of public domain compositions following recognition of their usefulness in treating the diseases. Of particular interest is use of doxycycline to treat diabetes and hypertension.
WO2013013061A1 Methods and compounds for treating cancer The invention includes, in part, methods and compounds for treating cancer including, but not limited to gliomas, melanomas, and neuroblastomas. In some embodiments of the invention, a glyceryltriacetate compound is administered to a subject in an amount effective to treat or prevent a cancer in the subject.
US20090306187 Modulators of Itch Ubiquitinase Activity The present invention relates to the identification of new drug targets for therapy of disorders including cancer. In particular, the present invention relates to inhibition of the E3 ubiquitin ligase, Itch, as a means for treating disorders. Furthermore, the present invention relates to the regulation of p63 and p73 stability in cells. In particular, the invention relates to the modulation of the regulation of p63 and p73 stability in cells through modulation of the expression or activity of Itch. Moreover, the invention relates to the use of Itch as a target for the development of agents capable of modulating p63 or p73 stability and especially agents capable of modulating the interaction of Itch and p63 or p73. Such agents may be useful in therapeutic applications including cancer treatment and modulation of skin differentiation.
WO2012098505A1 2-methoxy-pyridin-4-yl derivatives The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
WO2010060836A1 Arylcyclohexylethers of dihydrotetraazabenzoazulenes for use as vasopressin via receptor antagonists The present invention is concerned with arylcyclohexylethers of dihydro-tetraazabenzoazulene derivatives, i.e. arylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene derivatives of formula (I) wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in particular as Via receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
CN1803786A Red sage root water soluble ingredient derivative ERJT-12 and its application in cancer resistance The disclosed ERJT-12 as the derivative of water-soluble constituent of radix salvia miltiorrhiza is composed by natural 5-(3-hydroxypropyl)-7-methoxy-2-(3-methoxy-4- hydroxy)-3-benzo[b] furaldehyde. Wherein, this compound takes microtubule as target, has obvious growth inhibition to multiple human tumor cells, can block the MCF-7 cell on mitosis time, and restrains the polymerization of tubulin.
EP2340808A1 Synergic combination of phenylpropanoids, such as verbascoside or teupolioside, and mesalamine The present invention relates to the synergic combination of mesalamine with phenylpropanoids (verbascoside or teupolioside), obtained from plant cell cultures, and the pharmacological and nutritional use thereof for the prevention and treatment of inflammatory disorders of the digestive apparatus. In particular, the present invention relates to a pharmaceutical composition containing mesalamine and one or more phenylpropanoids, together with pharmaceutically acceptable excipients.
CA2443314C Method of imaging cell death in vivo A method of imaging apoptosis in vivo, using radiolabeled annexin, is described. Methods for tumor radiotherapy are also provided.
US20080085923 Thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer; use with other drugs such as aspirin, clodipogrel, prasugrel, cangrelor, Fragmin; himbacine derivatives Multiple stereoisomers of the heterocyclic-substituted tricyclics of the formula: or a pharmaceutically acceptable salt, solvate, or ester of said compound wherein R and the stereochemistry are illustrated in the structural formulas herein are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
CN102198133B Application of 8-difluoro methoxy fluoroquinolone and composition thereof to tuberculosis treatment The invention relates to an application of 8-difluoro methoxy fluoroquinolone and composition thereof to tuberculosis treatment. The aim of the invention is to provide a new treatment purpose of a compound shown as formula (I), or medicinal salt thereof, or hydrate thereof, especially application of a pharmaceutical composition utilizing the compound as an active component to tuberculosis treatment.
US7459482 Agent for treatment of cisplatin-resistant cancer Preparation of a lipophilic platinum complex being dissolved or suspended in an iodized poppyseed oil fatty acid ethyl ester is useful as an agent for treatment of cisplatin-resistant cancers.
CN101683347A Topical preparation containing pazufloxacin and steroidal anti-inflammatory drugs The invention relates to a topical drug administration preparation containing pazufloxacin and steroidal anti-inflammatory drugs. The preparation contains suspending agents, cosolvents, a buffer system, surfactants, osmotic-pressure regulating agents, bacteriostats, pH regulating agents, stabilizing agents and other pharmaceutically acceptable necessary accessories. The preparation is topically applied to eyes, ears or noses.
WO2010137620A1 Phenoxyethylamine derivative Disclosed is a phenoxyethylamine derivative having an excellent selective α1D adrenergic receptor antagonistic activity. Specifically disclosed is a compound represented by formula (I) [wherein each symbol is as defined in the description] or a salt thereof.
WO2011071565A1 Tgr5 agonists TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
CN1676126A Method for preparing anticancer, cancer-preventing ocean active medicine The present invention relates to a preparation method of anticancer cancer-preventing marine active medicine using 2,3-indol quinone as main component. Said preparation method includes the following steps: purifying artificial synthetic 2,3-indol quinone; weighing (by mass%) 10-20% of 2,3-indol quinone, 30-40% of lactose, 25-35% of microcrystal cellulose, 1-5% of calcium carboxymethyl cellulose, 1-5% of anhydrous silicic acid, 3-8% of carboxypropionyl cellulose and 1-3% of magnesium stearate; uniformly mixing 2,3-indol quinone, lactose, microcrystal cellulose, calcium carboxymethyl cellulose and anhydrous silicic acid, adding them into carboxypropionyl cellulose dissolved by isopanol, mixing the obtained granules with magnesium stearate, using wet granule method and tabletting to obtain tablet preparation. Besides, it can use medicinal starch and 2,3-indel quinone according to mass ratio of 1:1-10 and proper quantity of magnesium stearate, uniformly mix them and make them into capsule.
WO2008023157A1 Nitrogen containing heterocyclic compounds useful as m3-receptor modulators A compound of formula (I): Formula (I) having M3 receptor- antagonist activity or having both muscarinic receptor antagonist and β2-agonist activity; a composition comprising such a compound; the use of such a compound in therapy (such as asthma or COPD); and a method of treating a patient with such a compound.
EP1140962B1 Novel derivatives from the class of oleandomycin The invention relates to novel compounds from the class of the macrolide antibiotic oleandomycin of general formula (I) wherein R<1> has the individual meaning of -CH2CH3 group, of a fragment of formula (II), together with R<2> has the meaning of a fragment of formula (III) or together with R<4> has the meaning of a fragment of formula (IV) or a fragment of formula (V), R<2> together with R<3> has the meaning of a ketone or together with R<1> has the meaning of a fragment of formula (III), R<3> has the individual meaning of OH group or together with R<2> has the meaning of a ketone, R<4> has the individual meaning of a methyl group, or together with R<1> has the meaning of a fragment of formula (IV) or of a fragment of formula (V), R<5> has the individual meaning of hydrogen or a benzyloxycarbonyl group, R<6> has the individual meaning of hydrogen, a methyl group or a benzyloxycarbonyl group, to intermediates for the preparation thereof, to a process for preparing them as well as to pharmaceutically acceptable addition salts thereof with inorganic or organic acids.
US20100291182 Drug-Loaded Fibers Implants and methods for the delivery of a therapeutic agent to a target location within a patient's body are disclosed. The implants include a fiber comprising a polymeric material and having a diameter of up to about twenty microns, and a first therapeutic agent within the fiber. The therapeutic agent is substantially in particulate form. The implants are of a variety of configurations, such as individual fibers, yarns, ropes, tubes, and patches.
EP2276469A2 Alpha adrenergic receptor agonists for treatment of degenerative disc disease Effective treatments of pain and/or inflammation from degenerative disc disease and/or facet joint are provided. Through the administration of an effective amount of at least one alpha adrenergic agonist at or near a degenerative disc and/or facet joint, one can reduce, prevent or treat pain and/or inflammation caused by the degenerative disc disease and/or facet joint.
WO2013161980A1 Cyclohexanediamide derivative and use thereof for medical purposes The purpose of the present invention is to provide: a compound having an sEH-inhibiting activity; and a medicinal agent which has an sEH-inhibiting activity and therefore can exhibit a therapeutic effect and a prophylactic effect on chronic kidney diseases and pulmonary hypertension. The present invention provides a cyclohexanediamide derivative represented by chemical formula (1).
EP2103603A1 Method for producing pyrrolidine compound Provided is a method capable of efficiently producing a compound having a superior HSD1 inhibitory action and a compound useful as a synthetic intermediate therefor, with superior achievability of asymmetric synthesis (i.e., superior selectivity), superior yield, superior safety and superior industrial workability at a low cost. A method of producing a compound represented by the following formula [8]: or a salt thereof, or a solvate thereof, from a compound represented by the following formula [2]: or a reactive derivative thereof, or a salt thereof, or a solvate thereof.
WO2011093826A2 Effervescent formulations comprising cefaclor and clavulanic acid as active agents Present invention relates to effervescent formulations comprising cefaclor and clavulanic acid and/or pharmaceutically acceptable salts, hydrates, enantiomers, racemates, organic salts, inorganic salts, esters, polymorphs, crystal forms and amorphous forms and/or combinations thereof suitable for oral use in treatment of infectious diseases caused by resistant bacteria. Active agents, when dispersed in an effervescent matrix, have surprisingly provided a clear solution. The obtained solution form has eliminated the disadvantages that are present in the dosage forms known in the art and furthermore it provided various advantages by means of use and bioavailability.
WO2012030919A3 Composition and method for muscle repair and regeneration The invention provides methods for muscle repair or regeneration comprising administering therapeutically effective amounts of RAR agonists or stem cells that are pretreated with contact with a RAR agonist to a subject at a site of muscle damage. Additionally, the invention provides compositions comprising RAR agonist treated stem cells and methods of use of said cells for muscle repair or regeneration. In one embodiment, the stem cells are mesenchymal stem cells. In one embodiment, the RAR agonist is an RARϒ agonist. In one embodiment, administration of the RAR agonist is begun during a period of increased endogenous retinoid signaling in the subject resulting from incurrence of the damaged muscle tissue.
US20110182985 Solid Pharmaceutical Composition with Enhancers and Methods of Preparing thereof The present invention provides pharmaceutical compositions which are effective in providing therapeutically effective blood levels of a therapeutically active ingredient to a subject when administered to a gastrointestinal tract. In one aspect, the pharmaceutical compositions comprise a therapeutically effective amount of a therapeutically active ingredient; at least one water soluble enhancer, e.g., a medium chain fatty acid or a salt, ester, ether, or derivative of a medium chain fatty acid and has a carbon chain length of from about 4 to about 20 carbon atoms; and a saccharide.
CN102988360A Compound amino acid injection (15HBC) composition The invention relates to a compound amino acid injection (15HBC) composition. Each 1000ml of the compound amino acid injection composition contains 7-8g of isoleucine, 8-9g of valine, 3.5-4.5g of leucine, 4-5g of lysine or 5-6g of lysine acetate, 5-6g of arginine, 1-2g of histidine, 2-3g of methionine, 3-4g of serine, 3-4g of phenylalanine, 6-7g of proline, 1.5-2.5g of threonine, 3-4g of glycine, 0.5-1g of tryptophan and 0.05-0.25g of L-cysteine hydrochloride, and is characterized in that each 1000ml of the injection further contains 0.5-1g of lactic acid.
CN103204808A Biquinoline derivative, preparation method thereof and application thereof in preparing anticancer medicament The invention relates to a field of medicament and chemical, and concretely to a biquinoline derivative, a preparation method thereof and an application thereof in preparing anticancer medicament. The biquinoline derivative has a structure as shown in a formula I or formula II which is as shown in specification, wherein R is H, aliphatic diamine or saturated heterocyclic amines. The biquinoline derivative provided by the invention has a strong interacting with guanine-rich telomeric DNA and c-kitDNA, is good in inhibitory activity for telomerase in cancer cells, thereby being substantial in inhibitory effect on cancer cell strains; and thus the biquinoline derivative is quite high in medical values and broad in market prospects.
CN101921224B 1-(3-aminopropyl) piperazine-4-aminoamide compound as well as preparation method and application thereof The invention discloses a 1-(3-aminopropyl) piperazine-4-aminoamide compound as well as a preparation method and application thereof. The structural general formula of the compound is shown as a formula I, wherein R1 is the following groups unsubstituted or substituted by 1-3 substituents: phenyl groups, benzyl groups, naphthyl groups, C5-C10 aromatic heterocyclic groups or C4-C7 saturated heterocyclic groups; the heterocyclic groups comprises 1-3 (at least 1) heteroatoms selected from N, O and S; the substituents are selected from the following atoms or groups: halogen, sulfydryl groups, hydroxyl groups, CF3, CN, NO2 and SO2CH3; and X is methylene, carbonyl or does exist. Through cell activity screening of an HIV-1 infected Bal(R5) lymphoid tissue sample, the series of compound is found to have very strong anti-HIV (Human Immunodeficiency Virus) activity, wherein the compound with strongest activity has the IC50 value reaching 10nM and the selection index more than 14.545 and can be developed into anti-AIDs medicaments. The formula I is shown in the specification.
EP1315491B1 Use of substituted pyrazoles for the manufacture of a medicament for the treatment of allergies A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles of formula (I).
EP1709052B1 Derivatives of 1,4-diazabicyclo 3.2.1octanecarboxamide, preparation method thereof and use of same in therapeutics The invention relates to compounds having general formula (I), wherein X represents N or a group having formula C-R2; P, Q, R and W each represent N or a group having formula C-R3; R1 represents H or an alkyl; R2 represents an alkyl; R3 represents H or a halogen, or an alkyl, alkoxy, nitro, amino, trifluoromethyl, cyano group, or having general formula -NR4R5, -NR4C ( =O ) R5, -NR4C ( =O ) NR5R6, - NR4C ( =O ) OR5, -NR4S ( = ) 2NR5R6, -OR4, -OC ( =O ) R4, -OC ( =O ) OR4, -OC ( =O ) ONR4R5, -OC ( =O ) SR4, -C ( =O ) OR4, -C ( =O ) R4, -C ( =O ) NR4R5, -SR4, -S ( =O )R4, -S ( =O ) 2R4, -S ( =O ) 2NR4R5, or a heterocycle; and R4, R5, and R6 each represent H or an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, or heterocycloalkyl or aryl. The invention also relates to the use of same in therapeutics.
US20120071437 Tunable crosslinked polysaccharide compositions The present specification generally relates to injectable dermal fillers including multifunctional polyethylene glycol-based crosslinking agents, hydrogel compositions comprising a matrix polymer crosslinked with such crosslinking agents, and methods of treating a soft tissue condition using such hydrogel compositions.
EP1071431B1 Cosmetic formulations comprising bis(triorganosilyl)hydroxycarboxylic acid derivatives The present invention provides greater than 99 % pure bis(triorganosilyl)hydroxycarboxylates of the general formulae: R3SiO-CHR1-COO-SiR¿3? and R3SiO-CHR?1-R2¿COO-SiR¿3? wherein each R is independently a monovalent straight or branched chain alkyl or alkenyl group having from 1 to about 6 carbon atoms, or an aryl group, R?1¿ may be hydrogen, a monovalent straight or branched chain alkyl group having from 1 to about 18 carbon atoms, or an aryl group, and R2 is a divalent straight or branched chain alkyl group having from 1 to about 18 carbon atoms, an aryl group, or a straight or branched chain alkaryl group having from 7 to about 18 carbon atoms; a process for producing the bis(trimethylsilyl)-hydroxycarboxylates comprising the trimethylsilylation with hexamethyldisilazane of the corresponding hydroxy carboxylic acids; cosmetic formulation comprising the greater than 99 % pure bis(trimethylsilyl)hydroxycarboxylates dissolved in aprotic media; and a method of delivering hydroxycarbxylic acids to the epidermis without apparent irritation or inflammation of the epidermis or stratum corneum.
EP1503714A4 Low profile combination device for gastrostomy or jejunostomy applications having anti-granuloma formation characteristics A combination device (1) for gastrostomy or jejunostomy usage having a retaining member (2), an elongated member (3) having a gastrostomy lumen (20) and a jejustomy lumen (22), and an inflatable balloon (26) mounted on the elongated member (3). The retaining member (2) is of a low profile and is arranged to be located on the skin adjacent a stoma in the abdominal wall through which the elongated member (3) extends. The balloon (26) seals the stoma about the elongated member (3). The retaining member (2) includes at least one access port (14/16) to communicate with respective ones of the lumens. The device (1), related compositions, and processes can prevent and/or treat granulomas.
CN101254177A Dantrolene sodium chewable tablet and method of preparing the same The invention provides a telbivudine chewable tablet for oral administration, and a preparation method and uses thereof. The telbivudine chewable tablet comprises telbivudine as active ingredient and pharmaceutically-acceptable adjuvants including bulking agent, adhesive, correctant and lubricant. The inventive telbivudine chewable tablet has the advantages of good mouthfeel, convenient administration, quick absorption, improved bioavailability and quick action.
CN1562019A Corydalis B long-acting preparation and its preparing method A slowly-releasing (or release-controllable) corydalis B for treating the pain, headache and insomnia caused by internal diseases, menalgia, etc contains corydalis B and slowly-releasing auxiliaries.
CN103655537A Application of oleaceran for preparing medicament for promoting small intestine peristalsis The invention relates to an application of oleaceran for preparing a medicament for promoting small intestine peristalsis. Proved by a pharmacological experiment, oleaceran has a good effect of promoting small intestine peristalsis. The application of oleaceran for preparing the medicament for promoting small intestine peristalsis is firstly disclosed, and belongs to a new skeleton type. Oleaceran has strong small intestine peristalsis promotion performance, and has outstanding substantive characteristics. Simultaneously, oleaceran for preparing the medicament for promoting small intestine peristalsis obviously has substantial progress.
EP2214657A1 Compounds for treating demyelination conditions Therapeutic methods, therapeutic combinations and pharmaceutical compositions provided herein are useful for inhibiting demyelination, for delaying the clinical onset of a demylination condition, for inhibiting progression and/or reducing frequency of relapse of a demylination condition, and/or enhancing physical ability of a human subject having a demylination condition. Lacosamide is one of the active compounds.
CN101229137A Gatifloxacin freeze-dried powder injection and preparing method thereof The invention provides a gatifloxacin freeze-dried powder injection and a preparation method for the injection and the method comprises the following steps: weighing and putting raw and supplemental materials into an aseptic container according to a formula and adding injection water with the temperature of 70 to 80 DEG C, and adding lactic acid solution after the uniform heat preservation and stirring and obtaining mixed solution of raw and supplemental materials with the pH value of 4.0 minus or plus 0.5 after stirring; adding injection activated carbon, and standing the mixed solution after the uniform stirring and obtaining de-carbonized filter liquor after the filtration and carbon removal; diluting the de-carbonized filter liquor with injection water to a preparation amount, and filtering through a 0.45Mum and 0.22Mum compound micro-porous filtering film after stirring the filter liquor uniformly and filling the obtained filter liquor into a bottle and keeping an air outlet; freezing and drying the obtained filter liquor which is filled into the bottle; pre-freezing under minus 40 DEG C for 2 to 4 hours and then decompressing, emptying space and drying for 24 to 28 hours in the condition of minus 40 DEG C to 10 DEG C and finally drying under the high temperature of 35 DEG C for 6 to 8 hours.
EP2090177A1 Food products having enhanced cocoa polyphenol content The invention provides a dry cocoa mix having conserved concentrations of polyphenols, and in particular cocoa polyphenols. The method of this invention avoids the significant and detrimental polyphenol losses that occur during conventional manufacture by controlling the handling of ingredients in the batching process to provide a product containing a significant amount of the cocoa polyphenols present in the raw materials used to formulate the finished product. The cocoa polyphenol containing ingredient is partially defatted cocoa solids.
CN1935263A Nano carbon suspension injection The present invention relates to the field of medical tracer diagnosis reagent. The nano carbon is an ideal trancer. Said invention relates to a nano carbon suspension injection, and is characterized by that in said injection the carbon whose grain size is 80 nm is adopted, and the polyvinyl pyrrolidone (PVP-K30) suspension adjuvant is added, then the above-mentioned materials are undergone the processes of magnetic stirring, reflux and ultrasonic treatment so as to obtain the invented nano carbon suspension injection.
WO2013054822A1 1 - arylcarbonyl - 4 - oxy - piperidine compounds useful for the treatment of neurodegenerative diseases The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
CN103735635A Medicinal composition for treating cancers and leukemia The invention discloses a medicinal composition for treating cancers and leukemia and a preparation method and an application thereof. The medicinal composition is prepared from the following raw materials in parts by weight: 12-24 parts of calomel and 9-21 parts of indigo naturalis, wherein the combination of calomel and indigo naturalis is taken as active substance. The medicinal composition has a good effect in treating cancers and leukemia. The invention also provides an application of the medicinal composition.
WO2010111136A3 Aliskiren modulation of neurogenesis The disclosure provides compositions and methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis by use of a renin inhibitor in combination with one or more neurogenic agents. The disclosure also includes compositions and methods for stimulating or activating the formation of new nerve cells based on the application of a renin inhibitor in combination with one or more neurogenic agents.
CN1814246A Anti-tumor cancer-diminishing medicine and preparing method The invention discloses an external-applied anticancer, tumor-eliminating, pain- stopping medicine for curing cancer and the preparing method, prepared of the follow medicinal materials in weight shares: Impatiens balsamina leaf 75í½100 sharesú¼Cottonrose Hibiscus Leaf 75í½100 sharesú¼Rhubarb 75í½100 sharesú¼Glauber's salt 35í½50 sharesú¼Mongolian Snakegourd Root 35í½50 sharesú¼Turmeric Root 15í½30 sharesú¼Realgar 15í½30 sharesú¼Rhizoma Arisaematis 15í½30 sharesú¼Frankincense 10í½20 sharesú¼Myrrha 10í½20 shares and Moschus 1í½3 shares by the steps of: regulating the raw materials, removing impurites from Moschus and placing Moschus in a pestle and grinding into fine powder 100-120 mesh; grinding Realgar into fine powder 100-120 mesh, and airing; crushing Glauber's salt, Frankincense and Myrrha into fine powders 100-120 mesh at -10í½0íµ; cleaning Impatiens balsamina leaf, Cottonrose Hibiscus Leaf, Rhubarb, Mongolian Snakegourd Root, Turmeric Root, Realgar, and Rhizoma Arisaematis, drying them at 60í½80íµ and crushign them into fine powders 100-120 mesh; mxing these raw materials with bee honey into plaster. And it has characters of convenient to use, suitable for the medium- and late- stage patients with poor appetite, dyspepsia, and absorption obstruction, low cost, improving the immunity, and simple process and equipment.
WO2007077159A1 Imidazo (1,2-a)pyridin-3-yl-acetic acid hydrazides, processes for their preparation and pharmaceutical uses thereof The invention provides novel imidazo[1,2-a]pyridin- 3-yl-acetic acid hydrazides of formula (I) wherein R1, R2 and R3 have different meanings, and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. Compounds of formula (I) are useful for treating or preventing, in a human or non-human mammal, diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic processes for preparing said compounds.
WO2007143895A1 Supersaturated solution of gemcitabine hydrochloride and prepraration method thereof A stable supersaturated solution of gemcitabine hydrochloride, which is prepared by dissolving completely gemcitabine hydrochloride in a medium by heating it at pH 4-8 to give a supersaturated solution of gemcitabine having a concentrate of 15-45g/L.
US20100099747 Reduction of polyalanine-induced protein aggregates and toxicity by ubiquilin A method for decreasing cell death in a cell exhibiting aggregation of polyalanine-containing proteins. The method includes introduction of an expression vector to a host cell comprising a nucleotide sequence encoding ubiquilin, followed by maintaining the transformed host cell under biological conditions sufficient for expression and accumulation of the ubiquilin in the host cell, wherein overexpression of ubiquilin reduces sensitivity of cell stress induced by expanded polyalanine proteins.
CN102977126A Dual-indolizine substitutive derivative as well as preparation method and use thereof The invention discloses a dual-indolizine substitutive derivative as well as a preparation method and use thereof. The preparation method is characterized by comprising the steps of: adding indolizine compound substituted at a first bit, aldehyde and a catalyst into an organic solvent under a stirring condition; and completely reacting at 20-30 DEG C under protection of nitrogen to obtain the dual-indolizine substitutive derivative after post-treatment. The easily obtained material is adopted to prepare the dual-indolizine substitutive derivative. The dual-indolizine substitutive derivative is good in reaction selectivity, mild in reaction condition, simple in preparation process, and low in production cost.
WO2005061551A1 Carboxy-reduced derivatives of chondroitin sulphate, method of preparing said derivatives, application thereof as a medicament and pharmaceutical compositions containing same The invention relates to: carboxy-reduced and chemoselectively O-sulphated derivatives of chondroitin sulphate having formula (I), wherein R1, R2, R3 and R4 represent H or SO3M, n is an integer of between 0 and 200 and M is an alkali metal, said derivatives being isolated or in mixtures; the diastereoisomers of said derivatives; the preparation method thereof; the applications thereof as a medicament; and pharmaceutical compositions containing same.
EP1849471A1 Aminosugar, glycosaminoglycan or glycosaminoglycan-like compounds, and S-adenosylmethionine A composition for the protection, treatment and repair and for reducing the inflammation of connective tissue in mammals and a method for the protection, treatment of connective tissue in mammals by the administration of the composition. The composition includes at least two compounds selected from S-Adenosylmethionine (SAM), an aminosugar selected from the group consisting of glucosamine, glucosamine salts, glucosamine hydrochloride, galactosamine, N-acetylglucosamine, and fragments, mixtures or salts thereof, and a glycosaminoglycan or glycosaminoglycan-like compound selected from the group consisting of chondroitin, chondroitin salts, hyaluronic acid, glucaronic acid, iduronic acid, keratan sulfate, keratin sulfate, heparan sulfate, dermatin sulfate, PPS, sodium PPS, calcium PPS, oversulfated GAGs, and fragments, salts, and mixtures thereof. The composition optionally includes manganese which promotes the production of connective tissue matrix. The composition also optionally includes methyl donors or methyl donor cofactors, such as vitamin B12, vitamin B6, folic acid, dimethylglycine or trimethylglycine, and betaine.
CN101550098A 4-isothio-urea-butyronitrile hydrochloride and application of derivatives thereof The invention relates to a 4-isothio-urea-butyronitrile and derivatives thereof, and the structural formula is shown in the formula I and II. The 4-isothio-urea-butyronitrile and derivatives thereof provided by the invention have better inhibiting effect on human ovarian cancer cells, hepatocarcinoma cells, lung cancer cells and human gastric carcinoma cells, wherein IC50=4.69x10g/mL, 3.98x10, 2.12x10 and 3.31x10g/mL; and the 4-isothio-urea-butyronitrile and derivatives thereof can be applied in preparing anti-cancer drugs for resisting ovarian carcinoma, hepatocellular carcinoma, lung carcinoma and human gastric carcinoma cells.
WO2010113840A1 Solid pharmaceutical composition containing amorphous body of solifenacin Disclosed is a solid pharmaceutical composition which contains a stable amorphous body of solifenacin or a pharmaceutically acceptable salt thereof, said amorphous body can be suppressed in decomposition over time. The solid pharmaceutical composition is used for the purpose of providing a preparation of solifenacin or a pharmaceutically acceptable salt thereof to a clinical site. Specifically disclosed is a solid pharmaceutical composition which contains: an amorphous body of solifenacin or a pharmaceutically acceptable salt thereof; citric acid or a pharmaceutically acceptable salt thereof (excluding a calcium salt); and one or more stabilizers for the amorphous body of solifenacin, said stabilizers being selected from the group consisting of sodium pyrosulfite and pharmaceutically acceptable salts of ethylenediaminetetraacetic acid.
US20120172429 Permanently charged sodium and calcium channel blockers as anti- inflammatory agents The invention provides compounds, compositions, methods, and kits for the treatment of neurogenic inflammation.
CA2782927C Derivatives of novel peroxides, method of preparation thereof and use thereof in human medicine as well as in cosmetics for the treatment or prevention of acne The present invention relates to the use of compounds of the following general formula (I). It also relates to the method of preparation thereof and to the application thereof in therapeutics.
US8349891 Crystalline solids of a MetAP-2 inhibitor and methods of making and using same The disclosure is in part directed to crystalline forms of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol and variants thereof.
US7632871 Methods of making and methods of using antiseptic disinfectant, cosmetic and toiletries, medicine or food containing the same The present invention relates to methods for producing and using antiseptic disinfectant, cosmetic and toiletries, medicine or food and method for antiseptically disinfecting a cosmetic and toiletries, medicine or food. The cosmetic and toiletries, medicine or food contain an antiseptic disinfectant comprising 1,2-alkanediol with 5-10 carbons and a fragrance component, and the fragrance component enhances the antibacterial activity that the 1,2-alkanediol originally has against a broad range of strains.
CN102558178A Tabersonine derivative, pharmaceutical compositions, preparing method and medical application thereof The invention provides antineoplastic active ingredient tabersonine derivative, as is shown in formula (I), pharmaceutical compositions, and the preparing method and the medical application thereof.
WO2006018815A1 Piperazine derivatives as adrenergic receptor antagonists The present invention relates to alpha la and/or alpha id adrenergic receptor antagonists of formula (I). Compounds described herein can function as alpha la and/or alpha id adrenergic receptor antagonists and can be used to treat. diseases or disorders mediated through alpha la and/or alpha id adrenergic receptors. Compounds described herein can also be used to treat benign prostatic hyperplasia or related symptoms thereof. Compounds described herein can also be used to treat lower urinary tract symptoms associated with or without benign prostatic hyperplasia. Also described herein are processes to prepare the described compounds, as well as pharmaceutical compositions thereof and methods of treating benign prostatic hyperplasia or related symptoms thereof.
CN101317979A Tea particle for toothache The present invention relates to a tea particle for treating toothache. The present invention is characterized by extracting a concentrated thick solution from Chinese rhubarb, bamboo leaf, raw gypsum, gardenia, wolfberry bark and common canscora herb; evenly mixing the concentrated thick solution with crystal maltitol, glucose, menthol and spice; then granulating, drying and sterilizing mixture, thus obtaining the particle.
US20050143430 Catechol bioisosteres The present invention provides catechol bioisostere compounds which are potent inhibitors of protein tyrosine kinases (PTKs). The present invention further provides methods of inhibiting PTKs, for example receptor protein tyrosine kinases (RTKs), comprising administering the catechol bioisosteres. The catechol bioisostere compounds are useful in treating or preventing PTK-related disease states, particularly protein tyrosine kinase related disorders which are associated with defects in signaling pathways mediated by PTKs.
US20120095386 Composition and device structure for iontophoresis Device structure 100 for iontophoresis provides electrode 101 and electrically conductive layer 102. Electrically conductive layer 102 contains active ingredient D and basic water swelling methacrylate copolymer P1 and/or acidic water swelling methacrylate copolymer P2. Electrode 101 and electrically conductive layer 102 are placed into a hollow of backing 103 and electrode terminal 104 is connected to electrode 101 through backing 103. Adhesive layer 105 is set around backing 103, and liner 106 to be removed when using the device, is placed so as to cover the hollow of backing 103.
US6916817 Inhibitors of metalloproteinases Arylpiperazines of Formula I useful as metalloproteinase inhibitors, especially as MMP13 inhibitors.
US20090252714 Autoantigenes for Improved Diagnosis, Prognosis and Treatment of Inflammatory Neurological Diseases According to the invention, autoantibodies, the appearance of which is characteristic of neurological autoimmune diseases, especially multiple sclerosis, are detected and the respective autoantigens identified. It can further be shown that many of these autoantigens are expressed specifically in the brain. The identification of the autoantigens and autoantibodies is useful for diagnosis and treatment. A brain-specific expression of the autoantigens further emphasizes an important role of the antigens and antibodies in the origin and development of neurological autoimmune diseases.
US20120022133 Antisense modulation of cholesteryl ester transfer protein expression Antisense compounds, compositions and methods are provided for modulating the expression of cholesteryl ester transfer protein. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding cholesteryl ester transfer protein. Methods of using these compounds for modulation of cholesteryl ester transfer protein expression and for treatment of diseases associated with expression of cholesteryl ester transfer protein are provided.
EP1898937A1 Heparin coating of biological tissue The present invention discloses an in vitro method to provide biological t issue with a heparin coating comprising the following steps; linking a biotin reagent to biological tissue, linking an avidin reagent to the biotinylated biological tissue, and linking a heparin reagent to the formed layer of avidin on the biological t issue thus forming a heparin coating. The invention further discloses a heparin coating on biological t issue, the use of a heparin coating, and the biological t issue coated with a heparin layer according to the method.
CN103340854A Stable zolmitriptan tablet The invention relates to a stable zolmitriptan tablet, and in particular relates to a solid medicine composition which contains zolmitriptan and a pharmaceutically acceptable slat of the zolmitriptan, and an arbitrarily-selected pharmaceutic adjuvant, wherein the pharmaceutic adjuvant is one or more than one of saccharides, starch and a derivative of the starch, cellulose and a derivative of the cellulose, and a lubricant. The zolmitriptan tablet has good stability and is endowed with a plurality of good properties by using a method.
US7160879 Melanin concentrating hormone receptor ligands: substituted 2-(4-benzyl-piperazin-1-ylmethyl)- and 2-(4-benzyl-diazepan-1-ylmethyl)-1H-benzoimidazole analogues Melanin concentrating hormone receptor ligands (especially substituted 2-(4-benzyl-piperazin-1-ylmethyl)-1H-benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
US7307079 Treating acute and chronic pain and inflammatory, gastrointestinal, allergic, cardiovascular, skin, opthalmological, respiratory, nervous system, cognition and memory disorders, etc. The invention relates to a group of novel triazine derivatives which are ligands for human adenosine-A3 receptors, as well as to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient. The invention relates to compounds of the general formula (1) wherein Y represents a group of the general formula (A), (B) or (C) and all other symbols have the meanings as given in the description.
WO2010082661A1 1,5-ag-containing composition Disclosed is a composition for ameliorating postcibal hyperglycemia which comprises at least one member selected from the group consisting of 1,5-D-anhydroglucitol, 1,5-D-anhydrofructose and derivatives of the same. Also disclosed is a composition for ameliorating postcibal hyperlipemia which comprises at least one member selected from the group consisting of 1,5-D-anhydroglucitol, 1,5-D-anhydrofructose and derivatives of the same. The aforesaid composition for ameliorating postcibal hyperglycemia and composition for ameliorating postcibal hyperlipemia are appropriately usable for ameliorating the symptoms of postcibal hyperglycemia and postcibal hyperlipemia in those who have these symptoms or signs thereof.
CN101288645A Tilidine medicine resin oral turbid suspension and preparation method thereof The invention discloses a tilidine drug-resin oral suspension and a preparation method thereof. The tilidine drug-resin oral suspension comprises the following components: every 100ml oral suspensioin contains 0.2g to 5g of tilidine or the pharmaceutical acceptable salt or hydrate and 0.2g to 10g of ion-exchange resin, and water is added to 100ml. The invention further discloses a preparation method of the oral suspension. The invention carries out the ion-exchange reaction of the tilidine and the ion-exchange resin, thus forming a drug-resin complex, reducing the toxicity and the side effects of the drug and improving the stability of the drug; the ion-exchange resin can well shelter the bad smell of the drug active ingredient tilidine and lead the oral suspension to have good taste after the appropriate taste modification is carried out. The oral suspension has accurate fractional dose and is easy to be accepted by children, elderly people and other special patients as a liquid preparation; furthermore, the preparation method is simple, which can be realized by adopting an ordinary preparation device and be applicable to industrial production.
CN101269211B Shuangtang high calcium medicinal granule and preparation technique The invention aims at providing a low-sugar high-calcium medical granule and a production process. The low-sugar high-calcium granule includes zymolytic cattle bone powder, tuckahoe extract, milk protein, oligosaccharides, pumpkin powder, casein phosphoric peptide, vitamin and minerals. The absorptivity of the granule calcium is notably improved compared with the equivalent products, is in particular applicable for the diabetes sufferers to take for long time. The production process crushes and mixes the zymolytic cattle bone powder and the tuckahoe extract completely, so that the grease and the phlegm working against crushing in the mixture can be fully absorbed, and airflow ultramicro crushing technical process is available for obtaining calcium-source fine powder, the technical processis stable and is suitable for scaled industry production.
WO2014024195A1 A3 adenosine receptor ligands for use in treatment of a sexual dysfunction The present disclosure provides an A3 adenosine receptor (A3AR) ligand for the treatment of sexual dysfunction. In some embodiments the A3AR ligand is selected from an A3AR agonist and A3AR allosteric enhancer. The present disclosure also provides a method a method and pharmaceutical composition for treating a sexual dysfunction, the method comprises administering to a subject having the sexual dysfunction an amount of an A3 adenosine receptor (A3AR) ligand. In some embodiments, the A3AR ligand is an A3AR agonist and more specifically, IB-MECA.
CN103288615A Monocyclic phloroglucinol compounds and pharmaceutical composition and application thereof The invention provides monocyclic phloroglucinol compounds Rxd-20 and Rxd-44 or a pharmaceutical salt thereof, a pharmaceutical composition composed of the monocyclic phloroglucinol compounds serving as effective ingredients and at least one pharmaceutically acceptable carrier, a preparation method of the pharmaceutical composition and an application of the pharmaceutical composition in preparation of antineoplastic drugs. The Rxd-20 and Rxd-44 are phloroglucinol compounds with five-membered ring side chains, and have excellent cytotoxic activity in vitro, novel chemical structures and strong activity, thereby having more advantages if being used as the antineoplastic drugs.
DE102008052054A1 Cosmetic and/or pharmaceutical preparation, useful e.g. for hair care, hair cleaning and hair coloring, and for decorative cosmetics e.g. lipstick and for post-sun treatment or sanitary wipes, comprises dialkyl(ene) ether compound Cosmetic and/or pharmaceutical preparation, comprises dialkyl(ene) ether compound (I). Cosmetic and/or pharmaceutical preparation comprises dialkyl(ene) ether compound of formula (R 1>-O-R 2>) (I). R 1>, R 2>6-24 (preferably 12-18)C-alkyl- and/or alkenyl residue.
US20110236460 Therapeutic Implant Surgical implants of the present disclosed include a film comprising a first therapeutic agent and a mesh comprising a second therapeutic agent. The surgical implant includes a film in direct contact with a mesh. The first therapeutic agent may be released at a first rate and the second therapeutic agent may be released at a second rate.
CN101843634A Biocompatible dialysis fluids containing icodextrins The invention relates to a biocompatible dialysis fluids containing icodextrins. Glucose polymer-based solutions and methods of making same that can be used during medical therapy, such as dialysis therapy are provided. The glucose polymer-based solution preferably includes a first solution containing icodextrin at a pH ranging from about 1.5 to about 5.0 and a buffer solution at a pH ranging from about 7.0 to about 12.0 that are so constructed and arranged allowing the glucose polymer-based solution to be mixed prior to infusion into a patient. The glucose polymer-based solutions of the present invention can be made at physiologic pH and with minimal glucose degradation products.
US20120156164 In situ-forming hydrogel for tissue adhesives and biomedical use thereof Disclosed herein are an in situ-forming, bioadhesive hydrogel and the medical uses thereof. Being formed by in situ crosslinking through an enzymatic reaction, the hydrogel has an advantage over conventional bioadhesive hydrogels in terms of biocompatibility. In addition, the in situ-forming bioadhesive hydrogel has excellent biocompatibility and mechanical strength and has excellent tissue adhesiveness thanks to modification with/without dopa derivatives. The hydrogel finds a variety of applications in the biomedical field, including bioadhesives or hemostats, implant substances for tissue regeneration and augmentation, carriers for delivering biologically active materials or drugs, etc.
WO2014108832A1 Antibacterial oxazolone derivatives The invention relates to antibacterial compounds of formula (I): wherein U represents CH or N; V represents CH or N, provided that at least one of U and V does not represent N; R represents H, halogen, methyl, methoxy, cyano or ethynyl; either W represents a phenyl group substituted in para position with (C1-C3)alkyl, (C1-C3)alkoxy or (C1-C3)thioalkoxy and optionally in meta position with halogen, or W is a group having one of the formulae W1 and W2 below: W1 w2 wherein Q is O or S and X is CH or N; and salts of such compounds.
CN103214431A 2,3-dihydrobenzazapine*compound or its salt and its medical application The invention belongs to the pharmaceutical chemistry field, and relates to a 2,3-dihydrobenzazapine*compound with a structure shown in a formula I, the 2,3-dihydrobenzazapine*compound is capable of inhibiting glycogen synthase kinase-3beta(GSK-3beta), and is a small-molecule inhibitor of GSK-3beta, a non ATP competition effect mode is taken for inhibiting the activity of GSK-3beta, no obvious inhibition effect is provided on the tested various protein kinase, and the 2,3-dihydrobenzazapine*compound has high kinases selectivity, and can be used for preparing medicines for preventing or treating the diseases due to GSK-3beta abnormity. The invention further comprises an application of a pharmaceutically acceptable salt or a pharmaceutical composition of the compound for preventing or treating the relative diseases to GSK-3beta, the relative diseases to GSK-3beta are diabetes, Alzheimer's disease, stomach cancer, colorectal cancer, pancreas cancer, liver cancer or mixed acute leukemia, but the relative diseases are not limited by the above diseases.
CA2379585C Certain alkylene diamine-substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines Disclosed are compounds of formula (1), where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NNY receptors. These compounds are useful in the treatment of a number of CNSdisorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NNY 1 receptors and as standards in assays for NNY 1 receptor bindings. Methods of using the compounds in receptor localization studies are given.
WO2012123889A1 A synergistic pharmaceutical combination for the treatment of pancreatic cancer In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of pancreatic cancer comprising a CDK inhibitor selected from the compounds of Formula (I); and a compound capable of inhibiting epidermal growth factor receptor (EGFR) kinase activity. The present invention also provides a combination wherein said pharmaceutical combination useful for the treatment of pancreatic cancer further comprises gemcitabine. The present invention also provides a method for the treatment of pancreatic cancer in a subject comprising administering said pharmaceutical combination(s) to said subject.
CN102702068A 3-pyrrolo-cyclohexylidene-2-dihydroindolone derivative, and application of 3-pyrrolo-cyclohexylidene-2-dihydroindolone derivative The invention relates to a 3-pyrrolo-cyclohexylidene-2-dihydroindolone derivative and an application of the 3-pyrrolo-cyclohexylidene-2-dihydroindolone derivative. Biology experiments show that the compound or pharmaceutically acceptable salts of the compound have a function in adjusting the activity of protein kinase and are capable of inhibiting activity of a plurality of tyrosine kinases and synchronously inhibiting proliferation of a plurality of tumor cells.
CA2639247C Methods of enhancing the quality, nutritive and health values of meat from bovine The present invention relates to methods of increasing the selenium content in beef by feeding special enriched diets, methods of improving human immune function, such as providing anticancer benefits. The present invention further provides methods for improving the quality of beef meat through a special enhanced diet, wherein organic selenium, copper, zinc and manganese replace all inorganic and metallic forms.
WO2005000850B1 Novel crystalline forms of valacyclovir hydrochloride Provided are novel crystalline forms of valacyclovir hydrochloride denominated forms VIII, IX, X, XI, and XII and methods of making them. Also provided is a novel method for making valacyclovir hydrochloride in crystalline form V.
US20080280898 5-Bromo-1'-[(3-methyl-1H-inden-2-yl)carbonyl]spiro[indole-3,4'-piperidin]-2(1H); vasopressin receptor antagonist; antidepressant, anxiolytic agent; dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R5, R5′, X, Y and A are as defined in the specification.
CN103405681A Preparation method of lozenge for treating oral ulcer The invention discloses a preparation method of lozenge for treating oral ulcer. The lozenge is characterized in that raw materials include lindera aggregata, citronella, root of Kerr Treebine, black soya bean, cotton tree bark, semen coicis, hawthorn, chalcanthite, talc and vitamin C. The preparation method of the pharmaceutical composition comprises the following steps: extracting volatile oil of the lindera aggregata, the citronella and the root of Kerr Treebine for later use; adding the vitamin C and chalcanthite ultrafine powder into a water extract thick extract of the black soya bean, the cotton tree bark, the semen coicis and the hawthorn to uniformly mix; spraying the volatile oil obtained previously to prepare wet particles; and adding the talcum powder and uniformly drying and tabletting. Clinical application verifies that the lozenge can effectively treat oral ulcer, and the dosage form is well-accepted by patients, so that the lozenge is worth of applying and popularizing.
US20080227803 relieving and/or preventing side effects induced by a compound having opioid receptor agonism A compound represented by the formula (I): (wherein R1 denotes hydrogen or —CHRARB (wherein RA denotes a lower alkoxycarbonyloxy, cycloalkoxycarbonyloxy, acyloxy or a group represented by (where R2 denotes hydrogen or a lower alkyl with or without a substituent), and RB denotes hydrogen or methyl, or any of pharmaceutically acceptable salts thereof or any of solvates thereof.
CN1745747B Use of proanthocyanidin in preparing medicine for treating colitis An application of proanthocyanidin in preparing the medicines for treating ulcerative colitis and non-bacteria chronic colitis is disclosed.
US20120184558 Crystalline Salt Forms of a 5,6,7,8-Tetrahydro-1,2,4-Triazolo[4,3-a]Pyrazine Derivative This invention provides novel crystalline acid salt forms of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine, i.e. sitagliptin, to processes for their preparation and isolation, and to pharmaceutical compositions comprising the same.
US20080317669 Cloning of honey bee allergen C The present invention relates to a nucleic acid encoding a polypeptide capable of binding to IgE from subjects allergic to venom of an insect from the order Hymenoptera having a homology of more than 70% to the amino acid sequence of SEQ ID NO: 2, which is the honey bee allergen C (Api m 5). The invention further relates to expression vectors, host cells and polypeptides encoded by the nucleic acid, as well as diagnostic and pharmaceutical uses thereof.
EP1147103B1 Phenantrhridine-n-oxides with pde-iv inhibiting activity The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.
CN102160875B Blood-nourishing skin-moisturizing health product The invention provides a blood-nourishing skin-moisturizing health product, which is prepared from the following main raw materials in part by weight: 5 to 80 parts of Chinese angelica, 2 to 40 parts of seabuckthorn, 2 to 40 parts of processed rhubarb, 5 to 60 parts of sheep placenta, 2 to 40 parts of pine pollen and 0.1 to 10 parts of yellow wine. In the blood-nourishing skin-moisturizing healthproduct prepared, various medicines are compatible and synergic, beautifying functions are promoted mutually, the effects of nourishing blood, moisturizing skin, expelling toxin and beautifying features are better achieved, and the beautifying effect is obvious.
CN101278917A Method for preparing povidone iodine vaginal tablet The invention relates to a preparation method of a novel povidone-iodine vaginal tablet used for gynecological antisepsis and antiphlogosis, aiming at overcoming the disadvantages in prior variety, providing a novel formulation which has the advantages of broad spectrum, high performance, quick effect, stability and good compliance for a patient, which is used for vulvovaginal candidiasis, bacterial vaginosis and mixed infection vaginitis; and the invention has the advantages that a medicine is applied partially in vagina to avoid or reduce a possible untoward response of systemic administration; the effective concentration of the medicine in diseased region is high, thereby being good for playing a curative role; a PH buffer system added in the invention leads the PH of the medicine to be 3.5 to 4.0 which is similar to physiological PH in the vagina, thereby safeguarding the physiological environment of the vagina effectively, providing existence conditions which are suitable for beneficial microbial population in the vagina and promoting disease to recover.
CN101816671A Medicinal preparation containing leonurine salt and ammonium glycyrrhetate and application in treating chloasma The invention relates to a unit dosage preparation used for the combined delivery of leonurine salt and ammonium glycyrrhetate. The preparation can be used for treating chloasma. The invention also relates to a preparation method of the combined unit dosage preparation and an application of the combined preparation in treating the chloasma.
CN101897696A Sugar-lowering drug composition and application thereof The invention relates to a sugar-lowering drug composition and application thereof. The composition comprises 1) medicinal dosage of vildagliptin, 2) medicinal dosage of any one or combination of thiazolidinedione sugar-lowering drugs or medicinal salt thereof, sulfonylurea sugar-lowering drugs or medicinal salt thereof or biguanide sugar-lowering drugs or medicinal salt thereof and 3) B vitamins. The invention relates to application of the sugar-lowering drug composition to preparing the drugs for treating and/or controlling diabetes or diabetic complications. The composition can effectively overcome the defect that type 2 diabetes can not be controlled by singly taking the commonly used sugar-lowering drugs or vildagliptin in the prior art and simultaneously addition of the B vitamins is conductive to enhancing the treatment effect of the drug, effectively controlling the blood sugar, protecting the endothelial cell functions in a synergic manner, slowing rising of plasma homocysteine of the diabetes patients, especially the diabetes patients associated with chronic complications and reducing the diabetic complications.
EP1934224B1 Pyrazolopyrimidines as cyclin dependent kinase inhibitors for the treatment of cancer The present invention relates to Pyrazolo [1,5-a]pyrimidine compounds of formula III usefu as protein kinase inhibitors, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases such as, for example, cancer, inflammation, arthritis, viral diseases, neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, and fungal diseases (Formula III), wherein : R is an aryl substituted with one or more heteroaryl; R2 is selected from the group consisting of R9, alkyl, alkynyl, alkynylalkyl, cycloalkyl, -CF3, -C(O2)R6, aryl, arylalkyl, heteroarylalkyl, heterocyclyl, alkyl substituted with 1-6 R9 groups which groups can be the same or different with each R9 being independently selected, aryl substituted with 1-3 aryl or heteroaryl groups which can be the same or different and are independently selected from phenyl, pyridyl, thiophenyl, furanyl and thiazolo groups, (a), (b), (c) and (d), and heteroaryl substituted with 0-3 aryl or heteroaryl groups which can be the same or different and are independently selected from alkyl, phenyl, pyridyl, thiophenyl, furaπyl and thiazolo groups; R3 is selected from the group consisting of H, halogen, -NR5R6, -C(O)NR5R6, alkyl, alkynyl, cycloalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl, etc; R4 is H halo or alkyl.
US20080269304 Parakeratosis inhibitor, pore-shrinking agent and skin preparation for external use It is intended to provide a substance having an effect of shrinking pores by analyzing the mechanism of making pores perceptible and compositions such as a skin preparation for external use which exerts the above effect to thereby make pores imperceptible. As means for solving these problems, there are provided a parakeratosis inhibitor and a pore-shrinking agent comprising an antagonist to an excitatory cell receptor, for example, a glutamate receptor such as N-methyl-D-aspartic acid receptor or an ATP receptor such as P2X receptor, or an agonist to an inhibitory cell receptor such as a γ-aminobutyrate receptor such as bicuculline-sensitive receptor having the Cl-channel therein or glycine receptor, as well as a skin preparation for external use aiming at inhibiting parakeratosis and a skin preparation for external use aiming at shrinking pores each containing such an antagonist to an excitatory cell receptor or an agonist to an inhibitory cell receptor as described above. Owing to the effects of inhibiting parakeratosis and shrinking pores, the skin can be maintained in a healthy state without perceptible pores.
US7638134 Insertion sites in fowlpox vectors The present invention provides novel insertion sites for introducing DNA into pox vectors.
US20110021498 Indolyl- pyridone derivatives having checkpoint kinase 1 inhibitory activity Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, -AIk-N(R11)—R12, -0-AIk-N(R11)—R12, —C(═O)OH, carboxy-(C1-C3)-alkyl, or —C(═O)—NH—R13; AIk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(═O)—N(—R16)— or —N(—R17)—C(═O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring.
CN101791304A Application of Xyloketal B in preparing medicines for treating mitochondrial injury diseases The invention discloses application of Xyloketal B in preparing medicines for treating mitochondrial injury diseases. The Xyloketal B can inhibit mitochondrial membrane potential reduction and mitochondrial reactive oxygen cluster generation, protect the integrity of mitochondria and inhibit the release of cytochrome c, and can protect the mitochondria from being injured. The invention develops new medicinal application of the Xyloketal B and a new application field; and the Xyloketal B is safe without toxicity, and has strong pharmacological effects and better medicinal prospect.
US20090012141 Composition and Method for Making Oligo-Benzamide Compounds The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.
WO2007037627A1 Pharmaceutical composition comprising polysaccharides from angelica gigas nakai for prevention and treatment of cancer disease Disclosed is a pharmaceutical composition for prevention and treatment of cancers, comprising Angelan, a polysaccharide isolated from Angelica gigas Nakai, as an active ingredient, and a pharmaceutically acceptable carrier, excipient or diluents. In detail, Angelan is excellent in the inhibition of cancer cell growth and the suppression of attachment and invasion of cancer cells to extracellular matrix, thereby inhibiting metastasis of cancer cells. In addition, when Angelan is taken in combination with an existing anticancer drug such as doxorubicin, synergic anticancer effects can be obtained.
WO2008028963A2 Calreticulin for its use as a medication for the treatment of cancer in a mammal The present invention concerns the calreticulin for its use as a medication for the treatment of a disease in a mammal, said medication inducing an increased location of calreticulin at the cellular surface. Application for treating disease such as cancer.
US20100172976 Methods and compositions for inhibiting the function of polynucleotide sequences A therapeutic composition for inhibiting the function of a target polynucleotide sequence in a mammalian cell includes an agent that provides to a mammalian cell an at least partially double-stranded RNA molecule comprising a polynucleotide sequence of at least about 200 nucleotides in length, said polynucleotide sequence being substantially homologous to a target polynucleotide sequence. This RNA molecule desirably does not produce a functional protein. The agents useful in the composition can be RNA molecules made by enzymatic synthetic methods or chemical synthetic methods in vitro; or made in recombinant cultures of microorganisms and isolated therefrom, or alternatively, can be capable of generating the desired RNA molecule in vivo after delivery to the mammalian cell. In methods of treatment of prophylaxis of virus infections, other pathogenic infections or certain cancers, these compositions are administered in amounts effective to reduce or inhibit the function of the target polynucleotide sequence, which can be of pathogenic origin or produced in response to a tumor or other cancer, among other sources.
CN102875573A Cefixime compound and pharmaceutical composition thereof The invention relates to a pharmaceutical compound and in particular relates to a cefixime crystal compound. The cefixime compound is a crystal, and an X-ray powder diffraction pattern obtained by Cu-Kalpha ray measurement is shown as a figure 1. Main granularity of the cefixime compound crystal disclosed by the invention is 45-80Mum, and the distribution width is 30-100Mum. The cefixime crystal disclosed by the invention has high stability and high purity and is applicable to preparation of the pharmaceutical compound, and preferable dosage forms are dispersible tablets and granules.
CN101822672A Compound with metformin and repaglinide, preparation method thereof and application thereof The invention relates to a composite composition with metformin hydrochloride and repaglinide as active ingredients, a preparation method thereof and application thereof and belongs to the technical field of medicaments. The composite composition is a medicinal composition which is mixed by using the metformin hydrochloride and repaglinide as the active ingredients and by using a carrier and can be prepared into sustained-release tablets, sustained-release granules, sustained-release capsules, common troches and capsules, granules, dispersible tablets, chewable tablets, orally disintegrating tablets, buccal tablets, liquid capsules, soft capsules, drop pills and other oral preparations. The composite composition is used for treating patients with I-type diabetes or II-type diabetes (non-insulin-dependent diabetes) and has synergistic effect on controlling blood sugar.
US20090088430 hydroxysteroid reductase inhibitors such as 4-{(R)-3-[3,5-Dichloro-4'-(4-trifluoromethyl-piperidine-1-carbonyl)-biphenyl-4-ylmethyl]-2-oxo-pyrrolidin-1-yl}-piperidine-1-carboxylic acid methyl ester, used for treating diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia and metabolic syndrome The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
WO2012026565A1 Method for producing phenyl-substituted heterocyclic derivative by means of coupling method using a palladium compound The present invention provides a method for producing a xanthine oxidase inhibitor, which is a therapeutic agent for hyperuricemia, or intermediates of the same, said method being efficient and using a short-procedure. The present invention is a novel coupling method for obtaining a compound represented by formula (3) by bringing about a coupling reaction between a compound represented by formula (1) and a compound represented by formula (2), in the presence of a palladium compound, a ligand obtained by coordination in a palladium compound, a base, a C1-C40 carboxylic acid, and at least one kind of additive.
WO2010040254A1 The use of flavones from radix scutellariae in manufacture of medicaments for treating enterovirus infection The present invention discloses the use of baicalein, baicalin or total flavones extracted from Radix Scutellariae in manufacture of medicaments for treating enteric virus causing hand-foot-mouth disease. The active component is mixed with pharmaceutically acceptable carriers to formulated into preparations for treating or preventing hand-foot-mouth disease clinically.
CN103301112A Application for Aphanamgrandiol A in preparation of medicines for treating chronic obstructive pulmonary disease The invention discloses a novel application for Aphanamgrandiol A in preparation of medicines for treating chronic obstructive pulmonary disease. The application for Aphanamgrandiol A in preparation of medicines for treating chronic obstructive pulmonary disease is disclosed for the first time; Aphanamgrandiol A has a new framework type, and an unexpectedly high inhibitory activity for chronic obstructive pulmonary disease, so that the possibility of giving any revelation by other compounds is avoided; and Aphanamgrandiol A has prominent substantive features, and an obviously remarkable improvement in case of being used for resisting chronic obstructive pulmonary disease.
WO2012108490A1 Isoquinoline amide derivative [Problem] To provide an excellent therapeutic or prophylactic agent for dementia, schizophrenia, and the like, which is based on a serotonin 5-HT5A receptor-modulating action. [Solution] The present invention was realized by discovering that an isoquinoline derivative, wherein a ring group is bonded to position 1 of the isoquinoline ring and a ring group or the like is further bonded to position 7 of the isoquinoline ring via a linking group having an amide group, has a potent 5-HT5A receptor-modulating action and an excellent pharmacological action based on that action, and by finding that the derivative is effective as a prophylactic or therapeutic agent for dementia, schizophrenia, and the like.
CN102258613B Sophora alopecuroide skin bacteriostatic spray and preparation method thereof The invention provides a sophora alopecuroide skin bacteriostatic spray and a preparation method thereof. The preparation method mainly comprises the following steps of: (1) adding heartleaf houttuynia herb, szechuan lovage rhizome, rhubarb and schizonepeta spike into an extraction tank in a mixed way, and extracting by using ethanol to obtain total filtrate which is recorded as liquid A; (2) adding sophora alopecuroide into ethanol and soaking, performing reflux extraction, filtering remained filtrate and adding into the liquid A to obtain liquid which is recorded as liquid B; and (3) extracting volatile oil from angelica, pepper and cloves by using distilled water to obtain mixed volatile oil A and mixed extract, filtering and concentrating the mixed extract, performing alcohol precipitation, filtering, recovering alcohol to obtain filtrate, adding the volatile oil A and the filtrate into the liquid B, uniformly stirring and recording the liquid as liquid C, dissolving menthol and borneol by using ethanol and then adding into the liquid C, adjusting alcoholic strength, stirring, standing, filtering to obtain the filtrate, namely a finished product. The sophora alopecuroide skin bacteriostatic spray provided by the invention can be used for effectively treating common skin pruritus.
US7041699 Ascorbic compound; L-lysine compound; c) L-proline compound; and d) epigallocatechin gallate, epicatechin gallate, epigallocatechin, epicatechin, or catechin; blocking cancer proliferation and metastasis. A nutrient pharmaceutical formulation composition useful for treating cancer comprising ascorbic acid, L-lysine, L-proline and at least one polyphenol compound selected from the group consisting of epigallocatechin gallate, epicatechin gallate, epigallocatechin, epicatechin, catechin and the use of the composition in treating cancer and other tumors are provided.
WO2009021121A2 Identification and characterization of hcv replicon variants with reduced susceptibility to a combination of polymerase and protease inhibitors, and methods related thereto The present invention provides methods of decreasing the frequency of emergence, decreasing the level of resistance, and delaying the emergence of a treatment-resistant hepatitis C viral infection, by administering to a subject, either in combination or in series, an inhibitor of the hepatitis C RNA-dependent RNA polymerase NS5B, e.g., a benzofuran, such as 5-cyclopropyl-2-(4-fluorophenyl)- 6-[(2-hydroxyethyl)(methylsulfonyl)amino]-N-methyl-l-benzofuran- 3-carboxamide (HCV-796), and an inhibitor of the serine protease NS3, e.g., boceprevir. Additionally, the invention relates to methods of monitoring the course of treatment of a hepatitis C viral infection, methods of monitoring and prognosing a hepatitis C viral infection, and methods of identifying an individual with a decreased likelihood of responding to an anti-hepatitis C viral therapy. These methods use the sequence(s) of HCV nonstructural gene(s) to identify the emergence of a treatment-resistant hepatitis C viral infection, particularly a benzofuran (e.g., HCV-796) and NS3 inhibitor (e.g., boceprevir) treatment- resistant hepatitis C viral infection.
CN102250161A Irisone derivatives with tyrosinase inhibitory activity as well as preparation method and application thereof The invention discloses irisone derivatives with tyrosinase inhibitory activities as well as a preparation method and application of the derivatives, wherein the derivatives are represented by general formulas (I) and (II). An experiment demonstrates that the compounds can obviously reduce the activity of tyrosinase in a melanoma cell, reduce the biosynthesis level of melanin in a cell and inhibit the gene expression of tyrosinase mRNA. The irisone derivatives can be applied to the fields of cosmetics, pharmaceuticals and food and can be used as melanin generation inhibitors, skin whitening agents or food additives. The invention also discloses a method for preparing the compounds from Menispermaceae arcangelisia loureiri plant arcangelisia loureiri.
US20110288046 Analysis of sulfated polysacchrides The invention relates to methods and products associated with analyzing and monitoring heterogeneous populations of sulfated polysaccharides. In particular therapeutic heparin products including low molecular weight heparin products and methods of analyzing and monitoring these products are described.
US7652012 2-(R)-(4-fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide maleate and pharmaceutical compositions thereof The present invention relates to piperidine derivatives of formula (I) specifically 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide maleate and pharmaceutical compositions thereof, useful in the treatment of conditions mediated by tachykinins.
US20090221603 Heterocyclic amide derivatives as calcium channel blockers Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of heterocyclic amides are disclosed of the general formula (1) where Z is N or ═CHNR2 and X is NR2, O, S, S═O or SO2. Among other definitions for R, R1, W and Y, the compounds of formula (1) are further characterized by at least one of W or Y being CR3Ar2 where Ar is an aromatic or heteroaromatic ring (for example, where W or Y is a benzhydryl moiety).
CA2724020A1 Substituted quinazolines and their uses for myeoloprolific and thrombotic diseases This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treat-ment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utili-ty as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
WO2007024945A8 Condensed imidazolo derivatives for the inhibition of aldosterone synthase and aromatase The present invention provides a compound of formula (I): Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula (I) can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy. Finally, the present invention also provides a pharmaceutical composition.
US20120053236 Pharmaceutical composition for diabetic nephropathy and its preparation and application The invention relates to application of 4,4′-diphenylmethane-bis(methyl) carbamates (DPMC) extracted and isolated from Cortex Mori and preparation of medicine for diabetic nephropathy. The pharmaceutical composition is made up of DPMC as active ingredient and the normal drug carriers, and the weight percentage of active ingredient is 0.1-99.5%. For the remarkable effect of prevention and cure for diabetic nephropathy and convenience for use, it will be a new facultative drug for patients.
CN101678004A Triazol compounds for treating biofilm formation The present invention relates to the use of a compound of formula I, preferably 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid or a pharmaceutically acceptable salt thereof for the preparation of a medicament for use in the treatment of biofilm formation, e.g. of P. aeruginosa, e.g. in cystic fibrosis patients.
US20090142335 Methods of diagnosis and treatment of metabolic disorders The invention features diagnostic methods for metabolic disorders (e.g., diabetes and obesity), methods for screening for compounds useful in the treatment of metabolic disorders, and methods for treatment of metabolic disorders that involve sirtuin2.
WO2007029345A1 Tyrosinase activity inhibitor [PROBLEMS] To provide an excellent tyrosinase activity inhibitor. [MEANS FOR SOLVING PROBLEMS] A tyrosinase activity inhibitor which contains biotin or its derivative as the active ingredient; the above-described tyrosinase activity inhibitor which further contains ascorbic acid or its derivative; the above-described tyrosinase activity inhibitor which further contains vitamin E’s; and the above-described tyrosinase activity inhibitor characterized by being a solid preparation for internal use which contains one or more components selected from the group consisting of sweeteners and water-swelling substances. The above-described tyrosinase activity inhibitor is useful as a whitening composition.
CN102895301A Improved preparation technology of xylitol pills The invention discloses an improved preparation technology of xylitol pills, which comprises the following steps of: a. weighing the raw materials in parts by weight: 75-80 parts of xylitol, 5-10 parts of radix astragali, 2-5 parts of liquorice, 3-5 parts of platycodon grandiflorum, 1-3 parts of radix bupleuri and 5-10 parts of calcium gluconate; b. mixing the raw materials and then crushing, finely grinding, sieving to obtain fine particles of the mixed raw material, putting the mixture into a rotary drum and evenly stirring; c. putting the fine particles of the mixed raw materials at the temperature of 60-70 DEG C for 6-8 hours, melting, controlling the melting temperature to be 95-100 DEG C, cooling in a cooling spray chamber to 15-30 DEG C for e 1-3 hours; d. putting the cooled fine particles of the mixed raw materials into a mould for sizing to prepare the xylitol pills. The xylitol pills have the advantages that the calcium gluconate is beneficial to digestive absorption and supplementing calcium, and the liquorice, the platycodon grandiflorum and the radix bupleuri are used for preventing cold, so that the xylitol pills can better warm the stomach for patients with weak digestion and help to improve the immunity.
CN101333219B Penem derivates with mercapto pyrrolidine formamide benzene alkyl heterocycle The invention relates to a penem derivative containing sulfhydryl pyrrolidine formamide heterocyclic alkyl benzene as shown in general formula (I), and also relates to the easy hydrolysis esters of the derivative, the pharmaceutical acceptable non-toxic salts of the derivative, the isomers of the derivative, the hydrates of the derivative, as well as the hydrates of the esters or salts of the derivative; wherein, the detailed definitions of R1, R2, R3, R4, R5, R6, R7 and n are shown in the instruction book. The invention also relates to the preparation methods for the compounds in formula (I), the drug combinations containing the compounds in formula (I), as well as the purposes of the compounds in formula (1) as medicinal active substances, especially the applications of the compounds inthe preparation of drugs for curing and/or preventing infectious diseases.
US20080194656 Benzotriazole Derivatives as Cannabinoid Receptor Antagonists The present invention relates to a group of benzotriazole derivatives, infra that are potent cannabinoid-CB1 modulators (known as antagonists or inverse agonists), useful in the treatment obesity, psychiatric and neurological disorders, as well as other diseases involving cannabinoid-CB1 neurotransmission (Current Opinion in Drug Discovery & Development 2004 7(4):498-506) the pharmaceutically acceptable acid addition salts and stereoisomeric forms thereof, wherein R1 is hydrogen, halo, trifluoromethyl, C1-4alkyl, C1-4alkyloxy- or C1-4alkyloxycarbonyl; R2 is hydrogen, phenyl, C3-7cycloalkyl or C1-6alkyl optionally substituted with Ar1; R3 is hydrogen, hydroxyl or C1-6alkyl; Ar1 is phenyl or phenyl substituted with up to three halo substituents; and Het represents a monocyclic 5 or 6 membered partially saturated or aromatic heterocycle selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, pyrimidinyl, pyridinyl, pyrazinyl, triazinyl, pyridazinyl, 2H-pyranyl or 4H-pyranyl wherein said heterocycle is optionally substituted with C1-6alkyl;
US20120302576 Ampk modulators The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.
CN103601683A Benzohetercyclic compounds, preparation method thereof and applications thereof The invention provides non-nucleoside antiviral inhibitors, especially benzohetercyclic compounds shown by a general formula I or pharmaceutically acceptable salts thereof or hydrates thereof. The invention further provides a method for preparing the compounds or the pharmaceutically acceptable salts thereof or the hydrates thereof. Pharmacological tests show that the compounds or the pharmaceutically acceptable salts thereof or the hydrates thereof can effectively inhibit replication of hepatitis B virus DNA and hepatitis C virus RNA. Therefore, the invention further provides applications of the compounds in preparation of medicaments preventing and/or treating viral infection, especially the hepatitis B virus (HBV) infection and the hepatitis C virus (HCV) infection.
US20080300230 Use of extracts of the genus cimicifuga as organoselective medicines for treating diseases of the genitourinary tract caused by sex hormones The present invention relates to extracts from Cimicifuga species and particularly from Cimicifuga racemosa, which are suited for producing a ready-formulated drug for the selective treatment and/or prophylaxis of sexual hormone-related disorders of the uro-genital tract. The extracts in accordance with the invention are moreover suited for the treatment and/or prophylaxis of post-menopausal urinary bladder infections. They are furthermore indicated for the treatment of benign and malignant prostate hyperplasies.
EP1242408B1 Substituted bisindolylmaleimides for the inhibition of cell proliferation Disclosed are novel substituted pyrroles having formula (I). These compounds and their pharmaceutically acceptable salts are suitable for administration to patients as continuous infusion solution and are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds and methods for the treatment and/or control of cancer.
US20070287702 Thioridazine And Derivatives Thereof For Reversing Anti-Microbial Drug-Resistance The present invention relates to compositions comprising thioridazine, and derivatives thereof, together with antibacterials. These compositions have been found greatly enhance the activity of many classes of antibacterials, allowing the antibacterials to be administered at significantly lower doses. The thioridazine and the antibacterial act synergistically by pacifying the bacteria to the antibacterials. This synergistic affect lowering the inhibitory or effective concentration of the antimicrobials is most pronounced with the levorotatory isomer of thioridazine compared to the racemic or dextrorotatory isomer.
CN101024056A Method for preparing toxin-reducing bacteria vaccine for domestic animals, fowls The present invention discloses a preparation method of attenuated vaccine for livestock, poultry and aquatic animal. Said preparation method includes the following steps: mixing hypericin, astragalus root, pig's gallbladder, sihuanglian, licorice, lonicera flower and lesser galangal root according to a certain mixing ratio, cooking, condensing evaporated gas, drying to obtain powder, using ethyl alcohol solution whose concentration is 80%-90% to make extraction, adding cane sugar, water and anhydrous ethyl alcohol, mixing the above-mentioned materials with western medicine, uniformly stirring them so as to obtain the invented product.
CN102757442A Sulfur-substituted podophyllum derivative and synthetic method and application thereof The invention discloses a sulfur-substituted podophyllum derivative, and a synthetic method and application thereof. Through sulfur substitution reaction, 2-mercapto-1,3,4-thiadiazole or 3-mercapto-1,2,4-triazole is respectively introduced into a C-4 site of podophyllotoxin or 4'-demethyl-epipodophyllotoxin so as to obtain the sulfur-substituted podophyllum derivative represented by a formula (V). Cell apoptosis test results of in-vitro BGC823, HepG2 and A549 tumor cell strains show that sulfur-substituted podophyllum derivative has good anti-tumor activity, high safety and low toxicity and can be prepared into clinical anticancer medicines.
WO2008058988A1 Pyrrolo[1,2-a]imidazoledione effective in the treatment of peripheral neurotoxicity induced by chemotherapeutic agents The use of a compound of formula (I), is disclosed in treating and/or preventing 5 chemotherapy-induced peripheral neurotoxicity (CIPN). The invention includes pharmaceutical compositions wherein the compound of formula (I) is present in a mixture with anticancer agents. An improved anticancer treatment with reduced CIPN-related side effects is also provided.
US20090286852 RNA containing modified nucleosides and methods of use thereof This invention provides RNA, oligoribonucleotide, and polyribonucleotide molecules comprising pseudouridine or a modified nucleoside, gene therapy vectors comprising same, methods of synthesizing same, and methods for gene replacement, gene therapy, gene transcription silencing, and the delivery of therapeutic proteins to tissue in vivo, comprising the molecules. The present invention also provides methods of reducing the immunogenicity of RNA, oligoribonucleotide, and polyribonucleotide molecules.
US20130065848 Levoisovalerylspiramycin i, ii or iii, preparations, prepartation methods and uses thereof Disclosed are levoisovalerylspiramycin I, II or III, preparations, preparing methods and uses thereof. The preparations comprise levoisovalerylspiramycin I, II or III and pharmaceutically acceptable carrier and/or adjuvant, wherein the purity of levoisovalerylspiramycin I, II or III is above 90 wt %. The levoisovalerylspiramycin I, II or III has a good antibacterial activity, and the preparations include solution for injection, powder for injection or lyophilized powder for injection.
CN102101866A Halogenated derivatives of staurosporine, and preparation method thereof and use thereof The invention relates to halogenated derivatives of staurosporine, and a preparation method thereof and use thereof. In the invention, by starting from staurosporine (staurosporin), the compounds of the structure are prepared by chemical reactions. Experiments prove that the compounds have higher tumor cytotoxic activity and protein kinase C(PKC) inhibition activity and can be used as cell proliferation inhibitor or antitumor agent.
EP2671578A1 Prophylactic or therapeutic drug for peripheral neuropathy caused by anticancer agent An object of the present invention is to provide a drug which is effective for prophylaxis or therapy of peripheral nerve disorder occurred as a side effect of the administration of anti-cancer agents. The present invention is to provide a drug containing an ester of C10 fatty acid as an active ingredient for prophylaxis or therapy of peripheral nerve disorder induced by administration of a drug containing at least one of anti-cancer agents. The drug of the present invention containing the compound as an active ingredient is highly useful as a drug for prophylaxis or therapy of peripheral nerve disorder induced by administration of anti-cancer agents.
WO2006096913A1 A topical anaesthetic composition A method for providing anaesthesia to a subject having a wound, such as a laceration, a surgical incision, an ulcer, an abrasion or a burn, said method comprising the step of applying topically to the wound a composition comprising: at least one local anaesthetic agent; a hydrophilic or hydroalcoholic gelling agent; an antiseptic agent; a vasoconstrictor; and a detectable marker such as a food dye, wherein when the composition is topically applied to the wound of the subject the presence of the anaesthetic agent on the subject is indicated by the detectable marker. The method has been developed primarily for anaesthetising open wounds of animals, particularly those caused by husbandry procedures such as mulesing.
WO2012049550A1 Liquid pharmaceutical composition for pain treatment and prevention The invention relates to a liquid pharmaceutical composition in solution, formulated to be administered orally as drops, comprising the synergic combination of ketorolac and tramadol, as well as pharmaceutically acceptable excipients, which can be used in the prevention and treatment of moderate to severe pain in paediatric patients without causing adverse side effects.
WO2010139253A1 Glycyrrhetinic acid ester derivative synthesis method and deoxoglycyrrhetinic acid ester compound A compound represented by formula II, a preparation method and uses thereof in treating liver damage, inflammation and so on are disclosed. A method for preparing glycyrrhetinic acid derivatives are also disclosed. In the compound represented by formula II, R1 is H, linear or branched C1-C18 alkyl formyl, linear or branched C1-C18 alkenyl formyl or aryl formyl and R2 is linear or branched C1-C18 alkoxy or aryloxy.
US20100216847 Nornicotine for the treatment of pain This invention relates to the use of R(+)-, S(−)- or racemic nornicotine for the treatment of pain.
CN101940575A Cefditoren pivoxil solid preparation and preparation method thereof The invention relates to a cefditoren pivoxil solid preparation and a preparation method thereof, the preparation contains cefditoren pivoxil nano microcapsule and pharmaceutical adjuvant, wherein the nano microcapsule is prepared from cefditoren pivoxil and a carrier material according to the weight ratio of 4-8:1, and the carrier material is a combination of xanthan gum, silk fibroin and superfine silica gel powder based on a weight ratio of 1.5-4.5:1:1. By using the solid preparation and the preparation method thereof, an entrapment rate higher than 95% can be achieved, thereby avoiding burst release of the medicament, reducing the untoward effects and improving the compliance of patients.
WO2008107176A1 Meta-substituted phenyl sulfonyl amides of secondary amino acid amides, the production thereof, and use thereof as matriptase inhibitors The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.
US20130189240 Composition containing pias3 as an active ingredient for preventing or treating cancer or immune disease The present invention relates to a composition containing PIAS3 as an active ingredient for the prevention or treatment of cancer or immune disease. More specifically, the present invention relates to a composition containing the PIAS3 gene or an expressing protein thereof as an active ingredient for the prevention or treatment of cancer or immune disease, to an immunosuppressant composition, to a method for reducing or inhibiting undifferentiated T cells into Th17 cells using the PIAS3 gene or an expressing protein thereof, and to a method for activating regulatory T cells.
EP1280795B1 N-substituted carbamoyloxyalkyl-azolium derivatives N-substituted carbamoyloxyalkyl-azolium derivatives of general formula (I), wherein Q, Y, R?1, R2, R3¿, Y and X- are as defined in the claims and the description as well as salts, hydrates or solvates thereof. The compounds of the present invention have antifungal activity and are useful for the treatment of fungal diseases.
WO2006063762A1 Dipeptide nitriles The present invention is directed to novel salts and modifications of N-[1-(cyanomethylcarbamoyl)-cyclohexyl]-4-(4-propyl-piperazin-1-yl)-benzamide, their use in medicine, processes for their preparation and their use in the manufacture of pharmaceutical preparations.
WO2014160153A1 Treatment of a diastolic cardiac dysfunction with a trpv2 receptor agonist Described herein are inventions directed to methods of treating a diastolic cardiac dysfunction and the symptoms thereof in a subject that includes administering an amount of a TRPV2 receptor agonist effective to treat the diastolic cardiac dysfunction. The TRPV2 receptor agonist may be administered in at least one of an injection, orally, or transdermally. The amount of TRPV2 receptor agonist is sufficient to result in an improved performance on quantitative diagnostic criteria. In an embodiment, the TRPV2 receptor agonist is administered over a period of about 8 hours to about 24 hours. The TRPV2 receptor agonist may be used for short term treatments, i.e., less than a week, or it may be administered in a long term manner, i.e., over a period of weeks, months, or even years. Exemplary TRPV2 receptor agonists include probenecid, 2-aminoethoxydiphenyl borate, cannabinol, cannabidiol, and combinations thereof.
US6894067 5-heteroatom-substituted pyrazoles The present invention relates to 5-heteroatom-substituted pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.
CN101757209A Chinese and western compound medicine for preventing WSSV disease of penaeid shrimps The invention discloses Chinese and western compound medicine for preventing WSSV disease of penaeid shrimps, which relates to compound medicine which is applicable to curing diseases of aquatic animals and penaeid shrimps. The Chinese and western compound medicine of the invention is prepared with the following components by weight parts: 20 to 40 parts of rhizoma coptidis, 50 to 70 parts of scutellaria, 50 to 70 parts of phellodendron, 35 to 55 parts of gardenia, 2 to 8 parts of astragalus polyose, 10 to 30 parts of glucurolactone and 5 to 15 parts of vitamin C. The product of the invention plays the dual roles of anti-bacteria, anti-virus and organism conditioning, effectively solves the WSSV of the penaeid shrimps caused by a plurality of reasons, and is characterized by significant curative effect in preventing the WSSV disease of penaeid shrimps and no any toxic and side effect.
US20100080799 Wstf regulates the dna damage response of h2a.x via novel tyrosine kinase activity The present invention relates to methods of detecting and regulating cellular DNA damage as well as methods of screening compounds suitable for modulating cellular DNA damage. The methods of the present invention utilize antibodies that selectively bind to a phosphorylated tyrosine residue in a SQEY tyrosine phosphorylation motif sequence or a phosphorylated serine residue in a KENSSQ phosphorylation motif sequence, where the phosphorylated serine residue is closest to the glutamine residue. Also encompassed by the present invention are methods of treating a subject having cancer. These methods involve the administration of an agent that modulates the phosphorylation of the tyrosine residue in a SQEY motif. Suitable agents for modulating the phosphorylation of the tyrosine residue of the SQEY motif are also disclosed.
US20090221474 Histone deacetylases, and uses related thereto The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
WO2010132015A1 New compounds modulating gamma-secretase and their use in the treatment of alpha beta related pathologies, such as alzheimer's disease The present invention relates to novel compounds of formulae (I) and (II) and therapeutically acceptable salts thereof, their pharmaceutical compositions processes for making them and their use in therapeutic methods for treatment and/or prevention of various diseases. In particular, the invention relates to compounds which interfere with γ-secretase and/or its substrate and hence modulate the formation of Aβ peptides.
CN102872006A Applications of tagitinin a and derivatives thereof in treatment of metabolic diseases The invention provides novel applications of tagitinin A extracted from Tithonia diversifolia and derivatives thereof in treatment of metabolic diseases. The tagitinin A and derivatives thereof can be used for treatment of diabetes, regulation of blood sugar level and regulation of cholesterol and used for preparation of pharmaceutical compositions for treatment of diabetes, regulation of blood sugar level and regulation of cholesterol.
US20120264734 Aryl- or Heteroaryl-Substituted Benzene Compounds The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
EP2027105A2 Novel process for preparing intermediates of ccr antagonists The present invention relates to a novel process for the preparation of compounds of Formula (I) wherein X, Q, R1 and R2 are as defined in the specification, the compounds being useful in the preparation of therapeutic agents. The invention further relates to novel intermediates useful in the preparation of the therapeutic agents.
US20080051406 Brimonidine and timolol compositions Disclosed herein are compositions containing brimonidine and timolol. Therapeutic methods and medicaments related thereto are also disclosed.
CN1919174B Anticancer slow release agent including nimustine and its synergist Disclosed is a slow release injection for treating solid tumors which comprises slow release auxiliary materials and active anticancer constituents, wherein the active anticancer constituents includeNimustine or the combination of Nimustine and its synergists (such as Paclitaxe, camptothecine or cytophosphanel). The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved. The solid tumors include glioma, osteosarcoma, lymphoma, lung carcinoma, intestinal cancer, and breast cancer.
US20070066837 Podophyllotoxin derivatives as antitumor agents This invention relates to podophyllotoxin derivatives, more particularly to 4β-amino and 4β-amido derivatives of podophyllotoxin and 4′-O-demethylepipodophyllotoxin, which are useful for the treatment of tumors. Processes for the preparation of the compounds disclosed herein, pharmaceutical compositions containing these compounds, and methods for treating tumors are provided. The invention further relates to stereoselective compounds of podophyllotoxin and 4′-O-demethylepipodophyllotoxin derivatives.
WO2007026720A1 Ring-fused pyrazole derivative A ring-fused pyrazole derivative represented by the formula (1) or a pharmaceutically acceptable salt thereof: (1) wherein n represents 2 or 3; A represents the formula: -O- or the like; B represents a C1-10 alkylene group or the like; C represents a single bond or the formula: -O-; R1 represents a hydrogen atom, a pyrrolidinyl group or the like; R4, R5 and R6 independently represent a hydrogen atom, a halogen atom or the like; D1=D2 represents the formula: -CH=CH- or the like; E represents the formula: -O- or -NH- or the like; G represents a C1-10 alkylene group or the like; and R7 represents a hydrogen atom, a phenyl group or the like. The derivative or salt can inhibit the enzymatic activity of Lck involved in the abnormal activation of an immunocyte and is effective against the rejection in organ transplantation or an immune/allergic disease such as atopic dermatitis and asthma.
CA2204747C New azo derivatives of 5-aminosalicylic acid Compound of formula (I) and their salts and solvates are useful for the treatment or prevention of inflammatory bowel disease. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.
CN101926762A Rupatadine fumarate eye drops and preparation method thereof The invention relates to rupatadine fumarate eye drops. The eye drops are prepared from rupatadine fumarate serving as a primary medicament, and a thickening agent, buffer salt, an isotonic agent, a bacteriostatic agent and a solubilizer serving as auxiliary materials. A preparation method A comprises the following steps of: dissolving the thickening agent by using a certain amount of water, and dissolving the primary medicament, the buffer salt, the isotonic agent, the bacteriostatic agent and the solubilizer by using a certain amount of water for injection; and mixing the two kinds of solution, and adding a proper amount of water for injection to reach the needed concentration. A preparation method B comprises the following steps of: stirring the thickening agent, the rupatadine fumarate, the buffer salt, the bacteriostatic agent, the isotonic agent, the solubilizer and the water for injection for a long time until the solution is clarified; and supplying the water for injection to fix the volume. The rupatadine fumarate eye drops have the advantages of simple preparation method and use for treating ocular surface allergic diseases, and have the characteristics of obvious curative effect, no irritation, no toxic or side effect, high stability and the like.
CN1846771A Spot-eliminating and physique strengthening composition The spot eliminating and physique strengthening composition consists of wheat chlorine, protocyanidin, chitosan, aloin, nanometer level pearl powder and soybean isoflavone in certain weight proportion. It may be orally taken to regulate acid-base balance of human body fluid, eliminate endotoxin, replenish estrogen for women and reach other functions; and externally applied to eliminate toxin, nurse face, eliminate spots and beautify.
WO2006076318A1 Monopotassium salt of an ikb kinase inhibitor The present invention is directed to the compound of formula (II), or a solvate thereof. The invention is also directed to the pharmaceutical use of the compound as an IκB kinase inhibitor, crystalline anhydrous and hydrated forms of the compound, pharmaceutical compositions comprising the compounds of the invention, and stable pharmaceutical products comprising the compound. As an inhibitor of IκB kinase, the compound of the invention, functions via the selective inhibition of IKK, particularly an IKK-2 inhibitor; as well as exhibiting localized activity, as opposed to a systemic activity. Such an inhibitor is particularly useful for treating a patient suffering from or subject to IKK-2 mediated pathological diseases or conditions, e.g., asthma, rhinitis, chronic obstructive pulmonary disorder (COPD), or COPD exacerbations, that could be ameliorated by the targeted administering of the inhibitor.
CN103483158A Diphenylethane derivatives and application thereof The invention provides diphenylethane derivatives and application thereof. The diphenylethane derivatives comprise compounds disclosed as structural formula (I) and pharmaceutically acceptable salts thereof, wherein Rl is selected from alkyl group, cycloalkyl group, alkenyl group, alkynyl group, aralkyl group, aryl group, halogen or acyl group; R2 and R3 are respectively and independently selected from hydrogen, alkyl group, cycloalkyl group, aryl group, aralkyl group or acyl group; and R4, R5, R6, R7 and R8 are respectively and independently selected from hydrogen, alkyl group, alkenyl group, alkynyl group, aryl group, aralkyl group, cycloalkyl group, heterocyclic group, halogen, nitro group, cyano group, acyl group, amino group, amido group, hydroxy group, acyloxy group or alkoxy group. The embodiment of the invention also provides application of the derivatives in preparing medicines for treating immunological diseases, inflammations or autoimmune diseases.
EP2575774A1 Combination therapy methods for treating proliferative diseases The present invention provides combination therapy methods of treating a proliferative disease (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include the administration of an effective amount of at least one other agent that modifies the epigenetics in a cell.
US20110054028 Supplement for reducing hiv transmission and method thereof There is an urgent need for a method to reduce the risk of mother-to-child transmission (MTCT) of HIV during breastfeeding in HIV pandemic regions. The present invention provides a supplement for reducing the chance of transmitting HIV during MTCT and method thereof. The supplement comprising arachidonic acid (AA) alone, or a mixture of AA and DHA at safe intake doses. The supplement is provided to either the breastfeeding mothers or the babies to maintain cell membrane potential polarization through activation of the background potassium channels, thereby reducing the risk of HIV transmission.
US7442717 Compounds for treatment of sleep apnea, respiratory system disorders or kidney failure Novel substituted 2-aminoimidazoles of formula I, process for their preparation, their use as medicament or diagnostic aid, and medicament containing them. The compounds of this type are useful in the prevention or treatment of various disorders and can be employed inter alia for renal disorders such as acute or chronic renal failure, for disorders of biliary function, for respiratory disorders such as snoring or sleep apneas or for stroke
US20080119501 Immediate release oxymorphone compositions and methods of using same The present invention relates to compositions comprising oxymorphone or a pharmaceutically acceptable salt thereof and to methods of using such compositions to treat various conditions or disorders.
US20080107612 Anti-caries dental material A sustained-release, dental fluoride varnish material includes about 5 percent by weight of NaF; up to about 10 percent by weight of glycerin; up to about 5 percent by weight of fumed silica; and optionally, an amount of varnish additives selected from the group consisting of flavorants, rosins, gums and alcohols.
EP1794150A1 Benzimidazole derivatives and their use as cannabinoid receptor ligands I Compounds of Formula I, or pharmaceutically acceptable salts thereof: (I) wherein R1, R2, R3, R4, and R5 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
CN102885826A Application of Gypensapogenin B to preparation of drug for controlling liver injuries The inventor conducts pharmacological researches on Gypensapogenin B and finds that Gypensapogenin B has protective effects on mouse acute liver injuries induced by D-galactosamine (D-GalN) and CC14. Thus Gypensapogenin B can be used for preparing the drug for controlling liver injuries or hepatitis. The application of Gypensapogenin B to preparation of the drug for treating liver injuries is firstly publicized; and as a framework type belongs to a brand-new framework type, the framework type has unexpectedly strong activity on treatment of the liver injuries without any possibility shown by other compounds, and has outstanding substantial characteristics and remarkable progress for fighting the liver injuries at the same time.
US20080176939 Compounds which inhibit beta-secretase activity and methods of use thereof The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
WO2008130953A2 2-imin0is0thiaz0le derivatives as cannabinoid receptor ligands The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
EP2052720A2 Use of at least one hydroxylamine compound for the treatment of eye disease Uses for the treatment or prevention of a number of ocular diseases or disorders are disclosed. In particular, uses are disclosed for the amelioration of diabetic retinophaty and other retinopathies, as well as uveitis, presbyopia, dry eye, glaucoma, blepharitis and rosacea of the eye. The uses comprise administration of a composition comprising an ophtalmalogically acceptable carrier or diluent and a hydroxylamine compound in a therapeutically sufficient amount to prevent, retard the development or reduce the symptoms of one or more of the ophthalmic conditions.
WO2014052398A1 Inhibitor of beta-secretase The present invention relates to spirocyclic indane imidazole 4-amines and their use as inhibitors of the β-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.
EP2488645A1 Exon skipping therapy for dysferlinopathies The present invention relates to methods for restoring the function of a mutated dysferlin comprising the step of preventing splicing of one or more exons which encode amino acid sequences that cause said dysferlin dysfunction. Particularly, the splicing of exon 32 is prevented. The present invention also relates to a method for treating a dysferlinopathy in a patient in need thereof, comprising the step of administering to said patient antisense oligonucleotides complementary to nucleic acid sequences that are necessary for correct splicing of one or more exons which encode amino acid sequences that cause said dysfunction. Particularly, the splicing of exon 32 is prevented.
WO2011073339A1 Bicyclic thiazoles as allosteric modulators of mglur5 receptors The present invention relates to novel bicyclic thiazoles of formula (I) which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 ("mGluR5") and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.
US20070196385 Method of treating hepatitis C infection The present invention provides the use of PEG-IFN-α conjugates in association with ribavirin for the treatment of chronic hepatitis C infections. The present invention also provides a method for treating chronic hepatitis C infections in patients in need of such treating comprising administering an amount of PEG-IFN-α conjugate in association with an amount of ribavirin effective to treat hepatitis C.
CN101224223A Application of HCl in preparing medicine for treating gastritis, enteritis and vasculitis The invention relates to the application of chlorhydric acid in preparation drug for treating gastritis, enteritis and angeitis. The drug is water solution containing chlorhydric acid; the pH value of the solution is controlled within 1.5-6.9. The drug prepared by chlorhydric acid of the invention is safe and reliable and has exact and obvious effect on treating gastritis, enteritis and angeitis.
CN103127151A Application of Gypensapogenin A in medicines treating acute renal failure The invention relates to novel medical application of Gypensapogenin A, namely, application of the Gypensapogenin A in preparing medicines treating acute renal failure. The application of the Gypensapogenin A in preparing medicines treating acute renal failure is made public for the first time, due to the fact that matrix type is brand novel, besides, the Gypensapogenin A has an unexpectedly high acute renal failure inhibitory activity, the probability that inspiration is obtained from other compounds does not exist, and the Gypensapogenin A possesses outstanding substantial characteristics, meanwhile, significant progress is obviously achieved by the application of the Gypensapogenin A in resisting acute renal failure.
CN103494788A Pharmaceutical composition of rosuvastatin calcium tablets and preparation method of pharmaceutical composition The invention belongs to the field of pharmaceutical preparations and particularly relates to a pharmaceutical composition of rosuvastatin calcium tablets and a preparation method of the pharmaceutical composition. The pharmaceutical composition consists of an active medicine tablet core and a controlled-release layer wrapped outside the active medicine tablet core, wherein an alkaline substance calcium hydrophosphate is added in the tablet core, and the controlled-release layer consists of ethylcellulose, polyethylene glycol and polyacrylic resin III. According to the pharmaceutical composition, the stable and controlled-release rosuvastatin calcium tablets are obtained.
US20120157475 Combination Preparation Against Vertigo The use of cinnarizine and dimenhydrinate or their physiologically compatible salts in combination is described for the treatment of vertigo of any genesis.
US7994182 Quinazolinone-derivatives and their use for preparation of pharmaceutical compositions having PARP enzyme inhibitory effect The subject of the present invention are quinazoline derivatives and their pharmaceutically acceptable salts of general formula (I), that inhibit a DNA-repairing enzyme, poly(ADP-ribose) polymerase (PARP), enabling them to be used for the preparation of pharmaceutical compositions for preventing or treating illnesses where PARP-inhibition yields a beneficial effect. In general formula (I) R1 stands for either hydrogen or a group of general formula (a); R2 stands for a) hydrogen or C1-6 alkyl group, if R1 is other than hydrogen, and b) if R1 is hydrogen, then R2 may be a group of general formula (b), (c) or (d). The subject of the present invention also embraces the preparation processes of the compounds described above.
WO2010140817A2 Mineral composition and method of preparing same The present invention relates to a mineral composition and a method of preparing same. The method comprises the steps of: mixing 100 parts by weight of deep ocean water or deep sea water, Dead sea water, fossil salt water, marine deep water, peninsula deep water, coastal basement bedrock salt water, inland basement bedrock salt water, sea water, land salt water, mineral water, drinking water, fresh water, underground water or river water, water with salt melted therein with 1-15 parts by weight of seaweed, 0.1-10 parts by weight of a vegetable oil, 0.1-10 parts by weight of a soap from an animal fat, 0.1-10 parts by weight of a soap from a vegetable oil, 0.1-5 parts by weight of glycerin, 0.1-5 parts by weight of alcohol, 0.1-5 parts by weight of baking powder, and 0.1-10 parts by weight of salt; putting the mixture into a stainless tank equipped with a valve at a lower drain; heating the stainless tank to boil the mixture; adhering a material shaped into a plurality of wings or propellers to a stainless rod; mounting the stainless rod on an upper center of the stainless tank after installing the stainless rod on a electric motor; and rotating the stainless rod at high speed for 40-50 minutes with the wings submerged in salt water. By using the method, a lumped composition formed by the combination of minerals is separated from the salt water after seaweed, vegetable oil, soap, glycerin, alcohol, and baking powder are mixed with salt and broken down into fine particles. As the lumped mineral composition is not soluble in the salt water and is lighter than the salt water, the lumped mineral composition floats in the salt water and the salt water sinks. The cream-type mineral composition is obtained at this time when the valve is opened and the salt water is drained. Therefore, the mineral composition of the present invention can be effective in supplementing minerals as well as can be used for foods, cosmetics, medicines, and disease prevention.
US7118734 Non-aqueous liquid shampoo composition This invention relates to compositions suited to use as hair shampoos, and particularly those developed with a view to the treatment of a hair borne infestation, or of a skin disease of the scalp in addition to the primary purpose of hair cleaning and conditioning. In a first aspect of the invention there is provided a substantially non-aqueous liquid shampoo composition comprising at least one detergent, at least one active agent incompatible with water, an organic bulking agent and shampoo excipients, said organic bulking agent being miscible with water and miscible with said at least one detergent and shampoo excipients. It has been surprisingly found that replacing an aqueous bulking agent such as water with an organic compound which is compatible with active agents insoluble in water but which itself is miscible with water and miscible with detergents can produce a cosmetically and aesthetically acceptable non-aqueous liquid shampoo, particularly one having acceptable foaming characteristics.
WO2013076177A1 Salt of (r)-3-(6-amino-pyridin-3-yl)-2-(1-cyclohexyl-1h-imidazol-4-yl) ethyl propionate The invention relates to the salt of naphthalene-1,5-disulfonic acid with (R)-3-(6-amino-pyridin-3-yl)-2-(1-cyclohexyl-1H-imidazol-4-yl) ethyl propionate, which can be represented by the following structural formula of formula (I), to methods for the production thereof, to drugs containing said salt, and to the use of said drugs to treat diseases that are accompanied by thromboses, embolisms, hypercoagulability, or fibrotic changes.
WO2013017068A1 Substituted benzopyrone derivative and use thereof Disclosed are a substituted benzopyran derivative and the use thereof. The substituted benzopyran derivative has the structure of formula (I). It has been found in experiments that the derivative can be used to prepare drugs for treating psychotic conditions.
US7981899 Skin aging resistance, wrinkling resistance; (S)-1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid Disclosed are the use of compatible solutes for inhibiting the release of ceramides or for the prophylaxis and protection of human skin against premature skin aging and for the prophylaxis and protection of human skin against wrinkling.
WO2005009452A1 A composition for decreasing the risk of long-haul traveller’s syndrome comprising a mixture of pycnogenol and standardized giger root extract Use of Pycnogenol® and standardized ginger extract in a well-defined proportion (e.g. 1:1.5) in a newly invented combination product as a Health care composition with the trade name Zinopin®, targeting Long-haul Traveller's Syndrome in passengers travelling by air, land or sea is described. The active ingredients work synergistically to reduce the risk of Deep Vein Thrombosis and/or oedema associated with or without motion sickness. The mechanism of action of the combination in Long-haul Traveller's Syndrome is discussed in light of the established physiological effects of both as Generally Recognized As Safe (GRAS) active components. The innovative steps towards the development of Zinopin® and preferred dosage ranges and forms are discussed.
WO2014098232A1 Pharmaceutical composition comprising pi3 kinase inhibitor, pharmaceutical composition comprising compound which acts on vitamin d receptor, freeze-dried composition, method for producing freeze-dried composition, and pharmaceutical composition for transpulmonary administration A pharmaceutical composition which comprises a PI3 kinase inhibitor as an active ingredient. A pharmaceutical composition which comprises a compound that acts on a vitamin D receptor as an active ingredient. A freeze-dried composition of a composition which comprises a drug that has poor solubility to water, at least two kinds of amino acids, a surfactant, alcohol, and water.
US7241886 Method for preparation of 10,11-dihydro-10-hydroxy-5h-dibenz/b, f/azepine-5-carboxamide and 10,11-dihydro-10-oxo-5h-dibenz/b, f/azepine-5-carboxamide A method for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide and 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide from carbamazepine via a three-step process involving (i) epoxidation of carbamazepine; (ii) ring-opening of the resulting epoxide and (iii) oxidation of the resulting alcohol
US20120135969 Novel powdered crystalline medicines for inhalation The invention relates to manufacturing processes for preparing inhalable powders, and to the stable crystalline inhalable powders prepared by this process. Similarly, the invention relates to the use of these inhalable powders for preparing a medicament for the treatment of respiratory complaints, particularly for the treatment of COPD (chronic obstructive pulmonary disease) and asthma.
US20110306675 Compositions and methods for inhibiting nf-kb mediated tumorigenicity and adhesion-dependent survival of cancer cells Disclosed are compositions and methods for inhibiting NF-κB mediated cellular proliferation and metastasis. This abstract is intended to be used as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
EP1666047A1 Pharmaceutical compositions comprising nitric oxide-releasing pyrrolidones A polymeric composition capable of releasing nitric oxide under physiological conditions comprises a biopolymer bound to a nitric oxide releasing N2O2 - functional group of the formula: wherein J is a pyrrolidino group, bonded to N2O2 - by its nitrogen atom, M+x is a pharmaceutically acceptable cation, where x is the valence of the cation, a is 1 and b and c are the smallest integers that result in a neutral compound.
WO2007145868A1 Treating cystic fibrosis with antibiotics via an aerosol drug A method of treating respiratory disorders by delivering antibiotic to the lung alveoli using an aerosol drug delivery system.
CN1679942A Compound preparation of aspirin and ginkgo biloba extract and use thereof A compound medicine contains proportionally gingko extract, aspirin or composite aspirin, and pharmacologically acceptable additive.
CN1628682A Nanometer oleanolic acid powder for injection and preparation method thereof The invention provides a nano oleanolic acid powder for injection and preparation method, wherein the powder injection comprises the principal raw materials (by weight portion) of, active oleanolic acid 0.1-0.8, bean phospholipin 0.5-15 as carrier and/or poloxamer 1-20 as surface active agent, and freeze-drying adjuvant 60-750g.
US20090030088 Therapeutic benefits of gossypol, 6-methoxy gossypol, and 6,6'-dimothxy gossypol 6-methoxy gossypol and 6,6′-dimethoxy gossypol were isolated from cottonseeds. Bioactivities of these two gossypol derivatives and gossypol were investigated regarding their antioxidant activities, DNA damage prevention ability, anti-cancer, and anti-trypanosomal activities. Both methoxy compounds had nearly equivalent bioactivities, but gossypol showed greater bioactivities than either methoxy derivative on free radical scavenging activity, reducing power, and DNA damage prevention ability. Gossypol and its methoxy derivatives inhibited growth of three cancer cell lines, i.e., SiHa (cervical cancer), MCF-7 (breast cancer) and Caco-2 (colon cancer) cells, in a dose dependent manner. These three compounds also significantly inhibited growth of trypanosome T. brucei, the cause of African Sleeping Sickness, which affects thousands in western and central Africa.
CN103664897A Dihydropyrimidine compounds and application thereof in medicines The invention relates to dihydropyrimidine compounds and application thereof in medicines, particularly application in medicines for treating and preventing hepatitis B. Particularly, the invention relates to compounds disclosed as general formula (I) or (Ia), or enantiomers, diastereoisomers, tautomerides, hydrates, solvates or pharmaceutically acceptable salts thereof, wherein the variables are defined in the specification. The invention also relates to application of the compounds disclosed as general formula (I) or (Ia), or enantiomers, diastereoisomers, tautomerides, hydrates, solvates or pharmaceutically acceptable salts thereof, especially application in medicines for treating and preventing hepatitis B.
CN102086207A Camptothecin derivative with antitumor activity The invention discloses a camptothecin derivative with antitumor activity; the compound has good water solubility and highly-active antitumor effect, can be administrated orally and intravenously, and is applicable to antitumor therapy.
US20100130516 Purinyl derivatives and their use as potassium channel modulators This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
CN101590010A Mycophenolate mofetil intraocular medicament releasing system The invention relates to a mycophenolate mofetil intraocular medicament releasing system, which comprises mycophenolate mofetil. The system is characterized by also comprising a biodegradable macromolecule auxiliary material, wherein the mycophenolate mofetil and biodegradable medicinal macromolecule auxiliary material form a homogeneous mixture together; the weight ratio of the biodegradable macromolecule auxiliary material to the mycophenolate mofetil is 0.4:0.6-0.6:0.4; and the molecular weight of the biodegradable medicinal macromolecule auxiliary material is between 10,000 and 100,000 daltons. The biodegradable medicinal macromolecule auxiliary material is made of one of lactide-glycolide, polylactic acid, and polylactic acid-glycollic acid. The medicament releasing cycle of the system is a week or half a year, and the system has the advantages of little dosage, low drug administration frequency, high medicament utilization degree, high local concentration and lasting medicine effect, and reduction of the dosage of the whole body and the complications.
WO2013155341A1 Methods and compositions for treating ewings sarcoma family of tumors Compounds, compositions and methods relating to EWS-FLIl protein inhibitors are provided. The compounds have utility in the treatment of cancers including the Ewing's sarcoma family of tumors.
WO2008152094A3 Substituted acetamides as modulators of the ep2 receptor The present invention relates to substituted acetamides of the general formula (I), process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP2 receptor.
US7785620 Cholesterol lowering and blood lipids lowering composition The present invention is a composition containing cholesterol lowering and blood lipids lowering components such as phytosterols in a biologically easily available form in combination with unsaturated fatty acids or esters, short chain fatty acids or esters and/or hydrolyzed flour containing β-glucan and amylodextrin; food containing such a composition and a method for manufacturing of such a composition.
US20110070310 Topical ophthalmic pharmaceutical formulation of (2s,3s,4r)-n''-cyano-n-(6-amino-3,4-dihydro-3-hydroxy-2-methyl-2-dimethoxymethyl-2h-benzopyran-4-yl)-n'-benzylguanidine A topical ophthalmic pharmaceutical formulation may include particles of the compound (2S,3S,4R)—N″-cyano-N-(6-amino-3,4-dihydro-3-hydroxy-2-methyl-2-dimethoxymethyl-2H-benzopyran-4-yl)-N′-benzylguanidine suspended in a solution comprising monobasic sodium phosphate monohydrate, disodium phosphate heptahydrate, edetate disodium, benzalkonium chloride, sodium chloride, polysorbate 80, and water. A method of treating glaucoma may include topically applying to the eye of a patient in need thereof a therapeutically effective amount of this formulation.
EP2739639A1 Polymorphs of cddo ethyl ester and uses thereof The present invention relates to polymorphic forms of the compound of Formula (I) (i.e., ethyl 2-cyano-3,12-dioxoIeana-1,9(1l)-dien-28-oate (CDDO ethyl ester)) and methods of using them for treating a variety of disease states such as cancer and condisitons associated with inflammation.
US20090291955 Azacyclohexane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
US7317035 Tetracyclic arylcarbonyl indoles having serotonin receptor affinity useful as therapeutic agents, process for their preparation and pharmaceutical compositions containing them The present invention relates to novel tetracyclic arylcarbonyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel tetracyclic arylcarbonyl indoles of the general formula (I), their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention also relates to process/es for preparing such compound/s of general formula (I), composition/s containing effective amount/s of such a compound and the use of such a compound/composition in therapy
CN102875533A Dabigatran derivative, preparation method of dabigatran derivative and anti-thrombus application The invention relates to the field of pharmaceutical chemistry, in particular to a dabigatran derivative, a preparation method of the dabigatran derivative and anti-thrombus application. A pharmacodynamic test shows that the compound provided by the invention can achieve an anti-thrombus purpose by restraining thrombin, has certain restraining effects on adenosine diphosphate (ADP) and further strengthens anti-thrombus effect.
EP1599199A2 Methods for treating joint pain or improving sleep using an estrogen agonist/antagonist The present invention provides methods, pharmaceutical compositions and kits for treating joint pain and/or improving sleep using a SERM of formula (I): wherein the variables A, B, D, E, e, G, Y and Z 1 are as defined in the specification.
CN102532263A Bi-component drug micromolecule hydrogel based on hexadecadrol and taxol and preparation method thereof The invention relates to a synthesis and gluing method of bi-component drug micromolecule hydrogel precursors, which includes connecting an anti-inflammatory agent hexadecadrol and taxol through short peptide to form micromolecule hydrogel precursor molecules, and phosphate buffer solution (PBS) (pH=7.4) of the precursor molecules cuts off disulfide bonds under the effect of glutathione, dithiothreitol or the like to form hydrogel containing two drug components. The drug transmission system effectively overcomes the shortcoming of poor water solubility of the taxol, and the hexadecadrol serving as synergic drug of the taxol can effectively reduce toxic and side effects of the taxol.
CA2612265A1 2-substituted benzimidazoles Inhibitors of RSV replication of formula (I) the addition salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both -OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydro-thiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar2 or optionally subst ituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydro-furanyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl or 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; R3 is hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, cyanoC1-6alkyl, aminocarbonyl-C1-6-alkyl, mono-or di(C1-6alkyl)aminocarbonyl-C1-6-alkyl, carboxyl-C1-6-alkyl, C1-6alkoxycarbonyl-C1-6alkyl; R2 is hydrogen or C1-6alkyl; R3 and R4 are hydrogen, C1-6alkyl, Ar2, Ar2C1-6alkyl, C1-6alkylcarbonyl, Ar2carbonyl, Ar2C1-6alkylcarbonyl, C1-6alkylsulfonyl, aminosulfonyl, Ar1sulfonyl, Ar1C1-6alkylsulfonyl, C1-6alkyloxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)- aminoC1-6alkyl, hydroxyC1-6alkyl, aminocarbonylC1-6alkyl, C1-4alkyloxycarbonyl-C1-6alkyl, hydroxycarbonylC1-6alkyl, aminosulfonylC1-6alkyl, Het, Het-C1-6alkyl, Het-carbonyl, Het-sulfonyl, HetC1-6alkylsulfo nyl, Het-C1-6alkylcarbonyl; Het is an optionally substituted heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
CN101804056A Compound tablet of pioglitazone hydrochloride, glimepiride and preparation method thereof The invention relates to a compound tablet of pioglitazone hydrochloride, glimepiride and a preparation method thereof. The compound tablet contains sodium dodecyl sulfate and auxiliary with poor hygroscopicity, wherein the weight ratio of glimepiride to pioglitazone hydrochloride is 1-4:33; the content of sodium dodecyl sulfate by weight percent is 0.1-5%, and the content of the auxiliary with poor hygroscopicity by weight percent is 20-95%. The preparation method comprises the steps: the raw material of glimepiride, pioglitazone hydrochloride and the auxiliary with poor hygroscopicit are mixed into smashed mixing powder, the mixing powder, the raw material of pioglitazone hydrochloride, filler, disintegrant and lubricator are evenly mixed, and the mixture is subject to tabletting. The compound tablet solves the problems of imperfect dissolution of glimepiride, inferior stability and large industrialization difficulty of glimepiride. The preparation method according to the invention has the advantages of simple process, easy operation and better suitability for industrial production.
US20090263444 Fluocinolone Formulations in a Biodegradable Polymer Carrier Effective treatments of pain and inflammation are provided. Through the administration of an effective amount of fluocinolone at or near a target site, one can reduce, prevent or treat inflammation and pain and autoimmune disorders. In various embodiments, fluocinolone formulations may be provided within biodegradable polymers to reduce, prevent or treat sciatic pain and/or inflammation. In various embodiments, prevent transplant rejection for at least twenty-five days. In some embodiments, the pain relief can be for at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.
WO2013091285A1 Urea compound, preparation method and use thereof Provided are a urea compound having a structure as represented by general formula I, preparation method thereof, pharmaceutical composition containing the compound, and uses thereof in the preparation of drugs for treating inflammatory response, immune hyperactivity and organ transplantation rejection, wherein R1-R7, X, Y and n in the general formula are as defined in the specification and the claims.
US20080039421 Molecular Transporters Based On Alditol Or Inositol And Processes For The Preparation Thereof The inventive molecular transporter compound shows significantly high permeability through a biological membrane such as plasma membrane, nuclear membrane and blood-brain barrier, and accordingly, it can be effectively used in delivering various biologically active molecules, such as doxorubicin and paclitaxel to target cells.
WO2010008776A3 Crystalline form of (2s)-(-)-n-(6-chloro-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-sulfamide A patch and sensor assembly for use in an EP mapping system has two portions: a reusable portion and a disposable portion. The reusable portion houses the biosensors used in magnetic based location and mapping systems and the electrical lead necessary to communicate between the biosensor and the mapping system. The reusable portion may also contain a portion of the electrode necessary to receive electrical signals from the body of the patient. The disposable portion of the patch and sensor assembly contains an adhesive covered flexible patch having at least a portion of the electrode used to receive electrical signals from the body of the patient and may contain the electrical lead necessary to communicate such an electrical signal to the mapping system. The disposable portion contains a receptacle adapted to receive and mechanically secure the reusable portion to the disposable portion of the assembly. Such a patch and sensor assembly is useful in hybrid magnetic and impedance based location and mapping systems such as those used in electrophysiology.
WO2011134444A9 Substitution derivatives of n6-benzyladenosine-5´-monophosphate, methods of preparation thereof, use thereof as medicaments, and therapeutic preparation containing these compounds The invention relates to substitution derivatives of N6-benzyladenosine-5'- monophosphate of the general formula (I), wherein (R)n represents 1 to 4 substituents (n is in the range 1 - 4), which can be the same or different, and R is selected from the group comprising C1 to C8 alkyl, C1 to C8 alkoxy, amino, halogen, hydroxy, mercapto and nitro groups, and the pharmaceutically acceptable salts thereof. This invention also relates to methods of their preparation, their use as medicaments and in other applications, and a therapeutic composition containing these derivatives.
CA2237023C Improved formulation for administration of steroid compounds Improved cyclodextrin formulations for the administration of 5 .beta. steroids including a etiocholanolone, .beta. etiocholonolone, and etiocholandione are provided. Also provided are cyclodextrin formulations including at least one of the 5 .beta. steroids and DHEA. The formulations are suitable for parenteral administration, particularly intravenous administration and are also suitable for treating a condition which responds to treatment with the 5 .beta. steroids alone or together with DHEA, particularly where it is desired to decrease the amount of DHEA administered, including such conditions as obesity, diabetes syndrome, diabetes-associated hypercorticoidism or combinations thereof, anemic disorders including but not limited to aplastic anemia and anemia associated with renal failure or chemotherapy-induced or radiation-induced anemia or neutropenia, and autoimmune or inflammatory disorders such as lupus erythematosus.
US20070270403 Clozapine and Cocaine Effects on Dopamine and Serotonin Release in Nucleus Accumbens During Psychostimulant Behavior and Withdrawal The present invention provides methods of treating cocaine-induced pyschosis by administering an atypical antipsychotic compound in an amount sufficient to increase serotonin concentration in the nucleus accumbens of a mammal. According to the invention, atypical antipsychotic compounds include, without limitation, clozapine, risperidone, olanzepine, quetiapine, ziprasidone, sertindole, ketanserin, aripiprazole, and haloperidol, flupenthixol, thiroridazine, loxapine, fluspirilense, and sulpliride. The invention further provides methods for microvoltammetric imaging of changes in neurotransmitter concentrations in vivo and in real time comprising contacting the cell, cells, tissue, tissues, or organ of interest with a BRODERICK PROBE® sensor, applying a potential to said BRODERICK PROBE® sensor, and monitoring a temporally and spacially resolved recording using neuromolecular imaging (NMI) and electrochemical circuits such as, for example, voltammetry. In one embodiment of the invention, neuromolecular imaging may be performed before, during or after cocaine administration and/or cocaine-induced psychosis.
CN1765367A Vitamine U, belladonna and aluminiium dispersible tablet and its preparation process The invention provides an improved process for preparing vitamin U, belladonna and aluminium dispersible tablet by using vitamin U II, aluminum hydroxide and belladonna extract as raw material, starch as bulking agent, crystalline cellulose, sodium carboxymethylstarch, talcum powder and magnesium stearate as the auxiliary material.
WO2012160186A1 Oxygenated amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives and their medical use The present invention relates to oxygenated amino or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives, in particular the compounds of formula 1, 2, 3, 4, 5 or 6, and their medical use, including their use in the treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder, or a proliferative, neoplastic or dysplastic disease or disorder.
US20120232011 Use of Rapamycin and Rapamycin Derivatives for the Treatment of Bone Loss The present invention relates to a new use of rapamycin and rapamycin derivatives.
US20120022142 RNA Interference Mediated Inhibition of Signal Transducer and Activator of Transcription 1 (STAT1) Gene Expression Using Short Interfering Nucleic Acid (siNA) The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of STAT1 gene expression and/or activity, and/or modulate a STAT1 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against STAT1 gene expression.
EP2338484A1 Metabolic imprinting effects of structured lipids The invention relates to the use of triglycerides which an enhanced portion of the palmitic acid residues in the sn-2 position for an early in life diet for improving the development of a healthy body composition, in particular prevention of obesity, later in life.
US7087628 Heteroaryl and heterocyclic nitrogen ring containing hydrazide compounds useful for treating neurodegenerative disorderes This invention relates to a series of N-heterocyclyl hydrazides of Formula I, and pharmaceutical compositions containing them. The compounds of the invention have neurotrophic activity and are useful in the treatment and prevention of neuronal disorders such as Parkinson's disease, Alzheimer's disease, stroke, multiple sclerosis, amyotrophic lateral sclerosis diabetic neuropathy and Bell's palsy.
US6849632 Heteroaryl alkyl piperazine derivatives Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of diabetes, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.
US20100189650 Near-Infrared Responsive Carbon Nanostructures The present invention provides for compositions comprising carbon nanotubes (CNT) and gold (Au). The present invention further provides methods of manufacture of gold-carbon nanotubes (gCNT). The present invention provides methods of using gCNT for biological application.
WO2007092416A3 Melanin concentrating hormone receptor-1 antagonists The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula (I) wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
EP1228367B1 Aminophenoxyacetamide derivatives and pharmaceutical composition containing thereof There is provided an aminophenoxyacetamide derivative of the formula (I): wherein, R1 to R4 are, independent from each other, hydrogen atom; optionally substituted alkyl group; E?1 is -NR4- and E2¿ is oxygen atom or -NR10; Q is group -X-Y-Q' (X and Y are connecting bond; X is alkylene or alkenylene group, etc.; Y is selected from the groups consisting of C=O, NHC(=O), C(=O)NH, etc.; Q' is hydrogen atom or pheny, pyridyl groups which may be substituted, etc.),or a pharmaceutically acceptable salt thereof.These compounds have neuroprotective effect by introducing the CalbindinD-28k, one of Ca2+-binding proteins.11
CN102757420A Heterotactic aryl carboxylic acid compound, preparation method thereof, medicine composition comprising compound and application of compound The invention relates to a heterotactic aryl carboxylic acid compound as shown in a general formula I, a preparation method of the compound, a medicine composition comprising the compound and application of the compound, in particular to a novel compound synthesized by using heterotactic aryl as a framework and designing different substituent groups, a preparation method of the compound, a medicine composition comprising the compound and application of the compound to preparing medicines for treating obesity, diabetes mellitus, hyperlipidemia, hepatic steatosis and other metabolism-related diseases.
CN103330804A Medicine for treating pains and fevers of terminal cancer patients and preparation method thereof The invention aims to provide a non-narcotic medicine which can be taken for a long term and is used for treating pains and fevers of terminal cancer patients and a preparation method thereof. The medicine is prepared from the following raw materials in parts by weight: 10-20 parts of cinnabar, 9-30 parts of oyster shell, 10-20 parts of pseudo-ginseng, 10-25 parts of ginseng, 25-30 parts of glossy ganoderma, 18-30 parts of American ginseng, 9-12 parts of radix sophorae tonkinensis, 9-12 parts of red halloysite, 9-15 parts of barbary wolfberry fruit, 3-9 parts of pinellia tuber, 15-20 parts of radix astragali, 15-25 parts of glossy privet fruit, 15-20 parts of basic lead carbonate, 60-90 parts of gordon euryale seed, 10-20 parts of limonitum, 15-20 parts of Chinese yam, 10-25 parts of cinnamon and 150-200 parts of bitter wine. The preparation method is characterized by weighing the active pharmaceutical ingredients according to the ratio, putting the active pharmaceutical ingredients into an earthen pot, adding 1000ml of water to immerse the active pharmaceutical ingredients for 90 minutes, decocting the active pharmaceutical ingredients with soft fire for 60 minutes, filtering the decoction and taking the soup; then adding 800ml of water, decocting the active pharmaceutical ingredients with soft fire for 45 minutes, filtering the decoction and taking the soup; and combining the two soups and adding the bitter wine, thus obtaining the drug.
WO2008124128A2 Methods and compositions comprising desvenlafaxine or duloxetine for treating sleep-related breathing disorders Provided herein are methods of treating a sleep-related breathing disorder, such as obstructive sleep apnea, comprising the administration of O-desmethylvenlafaxine or duloxetine.
WO2004110419A8 Agonist agents and medicinal compositions It is intended to provide a medicine and a composition which make it possible to relieve or prevent fat and sugar metabolic errors such as fat accumulation, diabetes and hyperlipemia. Namely, an agonist agent to a peroxisome proliferator-activated receptor characterized by containing as the active ingredient a mono- or dicarboxylic acid having an isoprene skeleton structure in its molecule, a salt or an ester derivative thereof, a mono- or dialcohol having the above-described structure or an ester derivative thereof.
US20090221712 Mandelic hydrazides Novel mandelic hydrazides of the formula (I), in which R1-R11 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.
US7067536 phosphodiesterase 4 inhibitors in immunocompetent cells, such as macrophages and lymphocytes; side effect reduction; N-(3,5-dichloro-1-oxopyridin-4-yl)-[7-hydroxy-1-(3- or 2-nitrobenzyl)-indol-3-yl]glyoxylamide The invention relates to substituted 4-, 6- or 7-hydroxyindoles with N-oxide groups, process for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of phosphodiesterase 4 activity in particular in immunocompetent cells (e.g. macrophages and lymphocytes) by the compounds of the invention.
CN101601719A Emulsifiable paste for killing epiphyte The invention relates to an emulsifiable paste for killing epiphyte, belonging to a medical emulsifiable paste. The emulsifiable paste for killing epiphyte comprises the components of 0.02 percent of sodium monoflurophosphate (1), 3 percent of natural mint (2), 96.98 percent of high-quality talcum powder (3) and unlimited distilled water. The emulsifiable paste for killing epiphyte is characterized by being prepared from the components, has the advantages of simple prescription, easy production, low cost, stronger function of killing epiphyte, satisfied curative effect and no adverse reaction and is mainly used for hateable Hongkong foot and especially for the symptoms that the toes are itchy and very afflictive. The use method is as follows: firstly, the feet are cleaned and dried, and the emulsifiable paste for killing epiphyte is coated on the feet to relieve the worry and the symptom rapidly.
EP0873361B1 Crystals of the ligand-binding domain of the thyroid hormone receptor complexed to a ligand The present invention provides new methods, particularly computational methods, and compositions for the generation of nuclear receptor synthetic ligands based on the three-dimensional structure of nuclear receptors, particularly the thyroid receptor (herein referred to as 'TR'). Also provided are crystals, nuclear receptor synthetic ligands, and related methods.
EP2560971A1 Pyrrolopyridine inhibitors of kinases The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, Formula (I) wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
WO2008036021A1 Tetrahydro-lh-pyrido [3,4 -b] indole derivatives as cbl receptor ligands The present invention provides tetrahydro-lH-pyrido [3, 4- b] indole derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds act as cannabinoid receptor ligands (CB1) and thus may be used in the treatment of pain, cancer, multiple sclerosis, Parkinson's disease, Huntington's chorea, Alzheimer's disease, anxiety disorders, gastrointestinal disorders and/or cardiovascular disorders.
WO2009154651A1 Treatment of metastic breast cancer by a combination of two anti-her2 antibodies and a taxene The present invention concerns treatment of previously untreated HER2-positive metastatic breast cancer with a combination of a growth inhibitory HER2 antibody, a HER2 dimerization inhibitor antibody and a taxane. In particular, the invention concerns the treatment of HER2-ρositiv metastatic breast cancer in patients who did not receive prior chemotherapy or biologic therapy with a HER2 antibody binding essentially to epitope 2C4, a HER2 antibody binding essentially to epitope 4D5, and a taxane. The invention further comprises extending survival of such patients by the combination therapy of the present invention. In a preferred embodiment, the treatment involves administration of trastuzumab, pertuzumab and docetaxel.
CN101084915A Method for preparing nitrobenzoic oxycelluloseester for urea, creatinine adsorbent The invention discloses the structure, preparation method and application of a compound target adsorbent for oral administration--3, 5-dinitrobenzoic acid oxycellulose ester for treating chronic renal failure. The adsorbent for oral administration has a structural formula shown in (1).The preparation method comprises adopting microcrystalline cellulose as raw material, activating with alcali or ultrasonic wave, oxidizing C2 and C3 hydroxy of cellulosic glucose with oxidizer with high selectivity for synthesizing oxycellulose, carrying out reaction of C6 hydroxy of glucose and loops esterifying agent of nitrobenzene to obtain 3, 5-dinitrobenzoic acid oxycellulose ester; or adopting microcrystalline cellulose as raw material, adopting the oxidizer with selectivity and loops esterifying agent of nitrobenzene, and synthesizing 3, 5- dinitrobenzoic acid oxycellulose ester through microwave method. Specifically functional aldehyde group and nitrobenzene loop on 3, 5-dinitrobenzoic acid oxycellulose ester can generate Schiff reaction with -NH2 on urea respectively, generate jaffe complex reaction with creatinine and create steady 1:1 sigma complex compound, generate target adsorption with micromolecular urea and creatinine, and generate non-specifical physisorption, thereby scavenging toxin in patient of chronic renal failure, delaying the development of renal failure, and reducing the time of blood dialysis.
CA2176144C Anthracycline derivatives for treatment of amyloidosis The present invention provides the use in the manufacture of a medicament for use in the treatment of amyloidosis of an anthracycline of formula A: wherein R1, R2, R3 and X are appropriate substituents. Novel compounds of the formula A, processes for their production and pharmaceutical compositions containing them are also described.
WO2008039200A1 Methods and compositions for treating lymphoma and myeloma This invention relates to the use of antagonists of the hedgehog signaling pathway to induce apoptosis of lymphoma and myeloma cells and to treat subjects suffering from various forms of lymphoma or myeloma.
WO2011125006A3 Sultam compounds Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
WO2010033822A3 Therapeutic and diagnostic strategies The present invention encompasses the finding that microRNAs (miRNAs) regulate certain key proteins involved in DNA repair. In some embodiments, a miRNA suppresses levels and/or activity of one or more DNA repair proteins. In some such embodiments, such suppression renders cells hypersensitive to certain DNA damage agents (e.g., γ-irradiation and genotoxic drugs, among others). The present invention provides various reagents and methods associated with these findings including, among other things, strategies for treating cell proliferative disorders, certain diagnostic systems, etc.
CN1947719A Application of aspirin for preventing and treating osteoporosis An application of aspirin in preparing the medicines in the form of pill, tablet, particle, capsule, injection, etc for preventing and treating osteoporosis is disclosed.
CN101361741B New anti-tumor use of iso-oxazoline derivates The invention relates to the medicine field related to resistance to tumor and provides isoxazole oxazoline derivative with the structure of the general formula (1) and the pharmaceutically acceptable salt and the new application of the drug combination in preparing anti-tumor drugs, wherein, all the groups are defined as the specification.
CN103705797A Drug for treating kidney stones The invention provides a drug for treating kidney stones. The drug comprises the following drugs by weight: 30-40g of Indian bread, 30-40g of Chinese yam, 30-40g of asiatic cornelian cherry fruit, 10-20g of tree peony root bark, 15-20g of oriental waterplantain rhizome, 60-80g of prepared rhizome of rehmannia, 20-30g of plantain seed, 40-60g of christina loosestrife, 20-30g of Japanese climbing fern spore, 6-10g of akebia trifoliata var.australis, 15-30g of inner membrane of chicken gizzard, 6-10g of liquorice, 10-20g of talcum, 20-30g of giant knotweed rhizome, 40-60g of semen coicis, 1.5-3g of amber and 1.5-3g of potassium nitrate. The drug can eliminate or alleviate the symptoms of patients in 1-3 days, does not have toxic or side effect, is suitable for old and weak patients, has quite stable effects, can be used for dissolving and removing big and small stones from bodies, can be used for removing urinary tract stones and bladder stones, has the functions of tonifying the liver and kidneys, eliminating dampness and heat, treating stranguria and removing stones, and has the advantages of low cost, easiness in obtainment of drugs and the like.
US20100310477 Pharmaceutical compositions based on anticholingerics and additional active ingredients A pharmaceutical composition comprising an anticholinergic and at least one additional active ingredient selected from among corticosteroids, dopamine agonistes, PDE-IV inhibitors, NK1-antagonists, endothelin antagonists, antihistamines, and EGFR-kinase inhibitors, processes for preparing them and their use in the treatment of respiratory diseases.
US7335355 Antimicrobial agent A method of identifying an agent that enhances the anti-microbial activity of cationic anti-microbial peptides by blocking the inhibitory effects of the proteinase/glycosaminoglycan pathway, which method comprises: (i) providing, as a first component, a cationic anti-microbial peptide; (ii) providing, as a second component, bacteria; (iii) providing, as a third component, part of all of the components of a proteinase/glycosaminoglycan pathway such that the third component reduces the antimicrobial effect of the first component, for example, a glycosaminoglycan or bacteria or bacteria and a proteoglycan or a bacterial proteinase or a bacterial proteinase and a proteoglycan; (iv) contacting the first, second and third components with a test agent under conditions that would permit the killing of the bacteria by the antimicrobial agent in the absence of the third component, and that would permit the inhibition of the anti-microbial activity of the first component by the third component in the absence of the test agent; (v) monitoring the survival of the bacterial culture thereby determining whether the test agent is capable of enhancing anti-microbial activity wherein a test agent capable of enhancing anti-microbial activity promotes killing of the bacterial culture. Agents identified by such a method are useful in the therapy of acute and chronic infections, particularly in the treatment of ulcers and in the promotion of wound healing.
CN101301295A Use of compound pachymic acid for preparing medicament The invention relates to use of compound pachymic acid in the pharmaceutical field. The product has the functions of decreasing the rejection reaction of a receptor to a graft after a transplant operation, protecting the stability of haemolymph cell mitochondrial membrane potential at the periphery of the receptor, reducing the apoptosis percentage of haemolymph cells at the periphery, stabilizing the quantity percentage of CD8 + lymph cells at the periphery, and reducing the apoptosis percentage of the haemolymph cells at the periphery and regulating the quantity percentage of CD4 + and CD8 + lymph cells under nontransplant conditions and so on, is used to reduce graft rejection reactions as well as regulate and stabilize the quantity, the proportion and the function of the lymph cells of organisms during the transplant of organs, tissues and cells of animals and human beings and so on.
US20120087991 Mucositis prevention supplement and treatment The present invention provides for a nutritional composition comprising from 0.25 g to 25 g of glutamine, in neutral or salt form or precursor or derivative thereof; and from 0.1 g to 10 g of a phytochemical or a mixture thereof, wherein the phytochemical is an antioxidant. The nutritional composition is particularly useful in the treatment and/or prevention of mucositis.
US20080182983 degradation of hyaluronic acid and salt with hydrolase enzymes, to a form a mixture of tetrasaccharide, then applying the mixture to chromatography columns packed with ion exchangers and elution the tetrasaccharides; heat shock protein expression promoters, antiapoptosis, cell and tissue protectants Hyaluronic acid oligosaccharides having a size selected from sizes of 4 to 60 saccharides, fractions containing the hyaluronic acid oligosaccharides and having particular physicochemical properties, and drugs containing the same. The hyaluronic acid oligosaccharides of the present invention are extremely useful, because they exert superior pharmaceutical effects as active ingredients of a heat shock protein expression promoter, cell death inhibitor, cell injury inhibitor and cell and tissue protecting agent (e.g., organ preservation agent, antiulcer agent, antihepatopathic agent, IL-10 production promoter or IL-8 production inhibitor) and exhibit high safety.
CA2365079C Antiperspirant structured emulsion compositions An antiperspirant composition is a structured emulsion of a continuous phase containing water-immiscible liquid carrier plus a structurant, and a disperse phase which is a solution of antiperspirant active in water or a mixture of water and water-soluble solvent. The structurant is a fully or partially esterified saccharide. The compositions give low visible residue when applied to skin or to clothing.
US7037718 Mutant purine nucleoside phosphorylase proteins and cellular delivery thereof The present invention provides a procaryotic host cell stably transformed or transfected by a vector including a DNA sequence encoding for mutant purine nucleoside phosphorylase or hydrolase. The transformed or transfected procaryotic host cell can be used in combination with a purine substrate to treat tumor cells and/or virally infected cells. The present invention provides nucleotide sequences encoding mutant E. coli derived purine nucleoside phosphorylase proteins which can be used in conjunction with an appropriate substrate to produce toxins which impair abnormal cell growth. The invention provides for delivery of the toxin by generation within target cells or by administration and delivery to the cells from without.
EP1140024B1 Particles for oral delivery of peptides and proteins Microfabricated, asymmetrical, reservoir-containing particles for use in the oral delivery of biopolymer therapeutic agents such as peptides, proteins and oligonucleotides are disclosed. The particles are encapsulated in enteric-coated capsules or tablets to provide passage through the stomach and release of a suspension of the particles in the intestinal lumen. The particles have a selected shape, and uniform dimensions preferably in the 100 νm to 1 mm range. The reservoirs open to the face of the particle and are filled with a therapeutic agent and selected excipients. The excipients are selected to delay the dissolution/release of the agent from the particle reservoirs for 5-60 minutes after the particle is released in the intestinal lumen. Alternatively, the pore is plugged with an erodable material. The face of the particle is grafted with a layer of muco-adhesive ligands designed to quickly bind the particle to the intestinal mucosa for several minutes to several hours after release of the particles from the enteric-coated carrier.
WO2008070741A1 Compositions and methods for enhancing survival and reducing injury under ischemic or hypoxic conditions The present invention is directed to compositions and methods for enhancing the survivability of, and/or reducing damage to, cells, tissues, organs, and organisms, particularly under ischemic or hypoxic conditions.
WO2008024371A3 Multimediator transporter inhibitors for use in treatment of central nervous system disorders The invention provides a class of inhibitors according to formula (II), packaged Pharmaceuticals comprising such inhibitors, and uses of the inhibitors in treating, or the manufacturing medicaments for treating central nervous system disorders, including depression, anxiety, sleep disorders, obesity, attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), sexual dysfunction, substance abuse, and movement disorders. Related business methods, such as methods for conducting a pharmaceutical business and methods for conducting a medical assistance reimbursement program, are also provided. (II)
CN102225208A Limonene inclusion complex and preparation method thereof The invention provides a preparation method of a limonene inclusion complex, which comprises the following steps of: uniformly mixing 1 volume part of limonene and 1 volume part of 95% ethanol to obtain a mixed liquid; weighing 2 parts by weight of beta-CD (beta-cyclodextrin) based on the content of 1 volume part of limonene; dissolving 1 part by weight of beta-CD in 4-10 volume parts of boiling water, standing and cooling at room temperature; carrying out inclusion by using a colloidal mill method when the product obtained in the above step is cooled to 10-30 DEG C, and slowly adding the mixed liquid obtained in step 1; further adding 1 part by weight of beta-CD and continuing inclusion by using the colloidal mill method for 30-80 minutes to obtain an inclusion liquid; overnight standing the inclusion liquid at the temperature of 3-4 DEG C to separate into a solid layer and a liquid layer; and vacuum-filtering the inclusion liquid, washing filter cake with ethanol and drying under vacuum at room temperature to get the limonene inclusion complex. The invention also provides the limonene inclusion complex prepared by the preparation method.
EP1631146A4 Treatment of cancer with active vitamin d compounds in combination with radiotherapeutic agents and treatments The present invention relates to a method for treating cancer in an animal by administering to the animal an active vitamin D compound in combination with a radiotherapeutic agent or treatment.
CN102379889A Application of atemisia gmelinii extract in preparing drugs for preventing liver injuries The invention discloses a 2-hydroxyl-6-methoxy acetophenone-4-O-Beta-D-glucoside which is obtained by separating atemisia gmelinii and an application of acetophenone-4-O-Beta-D-glucoside and 6-methoxy-quercitin patuletin-7-O-Beta-D-glucoside in preparing drugs for preventing liver injuries. The active components of the drug of the invention are obtained by extracting and separating the atemisia gmelinii, the source of the active components is wide, and the liver injury curative effects are obvious.
CN103127109A Pharmaceutical composition containing dabigatran etexilate or salt and hydrate thereof The invention discloses a pharmaceutical composition containing dabigatran etexilate or salt and hydrate of the dabigatran etexilate. The pharmaceutical composition comprises an active substance pill core material containing the dabigatran etexilate or its pharmaceutically acceptable salt or hydrate and a filling agent and / or a bonding agent,and an organic acid or an organic acid material layer, the organic acid is arranged outside the active substance pill core materials, the organic acid material layer contains the organic acid, and the organic acid is selected from tartaric acid, succinic acid, citric acid, glutamic acid, fumaric acid, malic acid, aspartic acid or their hydrates or salts. After screening, the dabigatran etexilate active substance is prepared into a pill core, the organic acid material layer is added in an integrated mode, and meanwhile, an isolated layer is applied between the dabigatran etexilate active substance pill core and the organic acid material layer. The prepared dabigatran etexilate oral drugs composition has the advantages that solubility and dissolution rate are good, and bioavailability effect is prominent.
CN1907373A Plaster for covering ringworm of the nails The invention discloses a plaster for treating nail ringworm which comprises the raw materials of bee glue 30-50 parts, buthus martensi kirsch 5-10 parts, clove 15-25 parts, yellow corktree bark 10-20 parts, kuh-seng 15-25 parts, broom cypress fruit 10-20 parts, ganoderma lucidum 20-40 parts, wild pepper 20-40 parts, efflorescence 5-15 parts, nitric alkali 1-5 parts, acetic hyctro peroxide 1-5 parts, potassium permanganate 20-30 parts, iodine 150-200 parts.
WO2014113893A1 Use of galantamine and related compounds for treatment of inflammatory bowel diseases The invention provides for treatment of inflammatory bowel disease, including ulcerative colitis and Crohn's disease, through the use of muscarinic Ml receptor (MlmAChR) agonists. The agonists are capable of penetrating the blood-brain barrier and allow for central cholinergic activation of a vagus nerve-to spleen circuit. Central activation induced by muscarinic receptor agonist treatments reduced mucosal inflammation associated with decreased pro-inflammatory cytokine secretion by splenic dendritic cells (DC), mediated by oc7nAChR signalling.
CN101735237A Trimeric citrinin compounds as well as preparation methods and applications thereof The invention relates to preparation methods and applications of two trimeric citrinin compounds. In the invention, penicillium citrinum HGY1-5 which is collected from a crater sample is used for producing dimeric citrinin compounds in a novel structure. Experiments prove that the compounds can be used as a cell proliferation inhibitor, an apoptosis inducer or an antitumor agent.
WO2006105728A1 Diarylheptanoids, preparation and the use thereof The present invention provides diarylheptanoids , such as diphenyl heptanone , diphenyl heptenone , diphenyl heptanedione , and the use of pharmaceutical composition thereof for treating infection caused by helicobacter pylori or the diseases associated with ulcer in intestine and stomach . They have good effect on helicobacter pylori (Hp), and can restore mucous membrane lesions caused by helicobacter pylori .
CN102105436A Fatty acid derivatives for oral administration endowed with high paia- tability The invention relates to novel derivatives of short-chain fatty acids, in particular derivatives of butyric acid, useful for all the known clinical applications of the latter, which show physicochemical characteristics suitable for an easy oral administration, being devoid of the unpleasant organoleptic properties that characterise butyrate. The new compounds are amide derivatives which can be synthesised by reaction of the corresponding fatty acid halide with a naturally occurring amino acid, phenylalanine or a suitable derivative thereof, and which are in a poorly hygroscopic, easily weighable form, stable to acids and alkalis and able to release the acid at the small and large bowel level in a constant manner over time. They do not have disagreeable odours and are practically tasteless, thus allowing the manufacture of preparations for oral administration also suitable for the therapy of chronic diseases and in the paediatric field.
EP1527773A1 Pharmaceutical composition comprising sumatriptan The present invention relates to a pharmaceutical composition for oral administration capable of rapid disintegration and dispersion within the gastrointestinal tract comprising sumatriptan or a pharmaceutically acceptable salt or solvate thereof as active ingredient, in particular a composition in solid-dosage form that is intended to be swallowed, and methods of treatment of cephalic pain, especially migraine, using such composition.
CN101129676A Externally used plaster for treating bone disease and method of preparing the same The invention relates to an externally-used medicinal plaster for treating cervical vertebra diseases, hyperosteogeny, waist disc protrusion, periarthritis humeroscapularis, antirheumatic or rheumatoid arthritis and waist and knee strain, as well as the process for preparation, wherein the constituents include notopterygium root 1 part, dahurian angelica root 1. 5 parts, Clematis chinensis 1 part, Chinese angelica root 5 parts, cinnamon twig 1 parts, Cibotium barometz 1. 5 parts, long-nosed pit viper 1. 3 parts, dragon's blood resin 0. 4 part, licorice root 1 parts, lilac daphne 0. 5 part, radix salvia miltiorrhiza 0. 5 part, atractylodes rhizome 1. 5 part, Chinese ephedra 1. 5 parts, tuber of multiflower knotweed 1. 5 parts and radix salvia miltiorrhiza 6 parts.
US20070042971 Crystalline compound of 4'-demethyl-4'-phosphate-2", 3"-bispentafluorophenoxy-acetyl-4", 6"-ethylidene-beta-d-epipodophyllotoxin glucoside either in its free form or solvated with ethanol The invention relates to a crystalline compound of 4′-demethyl-4′-phosphate-2″,3″-bispentafluorophenoxyacetyl-4″,6″-ethylidene-β-D-epipodophyllotoxin glucoside in its free form or solvated with ethanol, advantageously provided in the form of a hemiethanolate solvate. The invention also relates to a method for preparing these compounds and to their use as an anticancer drug.
WO2008093979A1 Pharmaceutical composition for enhancing sexual activity comprising extracts from rhus verniciflua Disclosed is a pharmaceutical composition for enhancing male sexual function and treating male climacteric disorders, comprising a lacquer tree (Rhus verniciflua) flavonoid extract and/or anhydrous gallic acid separated therefrom as active ingredients. More specifically, provided is a pharmaceutical composition for enhancing male sexual function comprising, as active ingredients, flavonoids prepared by immersing Rhus verniciflua in a C1-4 lower alcohol or spirituous alcohol or extracting Rhus verniciflua with spirituous alcohol, and anhydrous gallic acid separated from the flavonoids via preparatory liquid chromatography. Since the pharmaceutical composition is derived from natural plants, it has no side effect and exhibits activities on the increase of testosterone, thus being useful as an active ingredient for foods as well as drugs for treating male climacteric disorders and enhancing sexual function.
CN103127004A Propylene glycol alginate sodium sulfate controlled-release granule and preparation method thereof The invention discloses a propylene glycol alginate sodium sulfate controlled-release granule and a preparation method thereof. The propylene glycol alginate sodium sulfate controlled-release granule comprises a quick release granule core and a controlled-release coating layer, wherein the quick release granule core comprises propylene glycol alginate sodium sulfate and a filler, the controlled-release coating layer comprises a controlled-release material, a plasticizer, a pore-foaming agent and an anti-sticking agent, and the propylene glycol alginate sodium sulfate controlled-release granule is prepared by wrapping the controlled-release coating layer outside the quick release granule core. The propylene glycol alginate sodium sulfate controlled-release granule is convenient to take, is slow to release, can achieve the purpose of increase of treatment effect for a long time, can reduce the dosage but maintains the same efficacy, thus reducing side effects on a patient caused by taking drug, being simple in preparation technology, obtaining products of stable quality, and being applicable to mass production.
CN103705484A Stable atorvastatin calcium tablet and preparation methods thereof The invention provides a stable atorvastatin calcium tablet which comprises a tablet core and a thin film coating, wherein the tablet core consists of atorvastatin calcium, filler, a disintegrating agent, a lubricant and a proper amount of a compound stabilizer, and the thin film coating contains a stabilizer. The invention further provides multiple preparation methods of the stable atorvastatin calcium tablet. The preparation methods comprise a wet granulation tabletting method, and the thin film coating is a water phase coating. The product is good in quality and high in stability, and the stable atorvastatin calcium tablet has the characteristics of simple process and suit for production on a scale.
CN101313925A Sanshi detoxication powder The invention discloses a three-stone alexipharmic pulverization for preventing and treating cloudy muscle disease of shrimps, which comprises the following materials in portion by weight: 15 to 40 portions of calcite, 5 to 15 portions of French chalk, 5 to 15 portions of plaster and 30 to 60 portions of cynanchum atratum. The three-stone alexipharmic pulverization has the characteristics of obvious effect and no toxic and side effect. The three-stone alexipharmic pulverization can be fed to shrimps remove various toxins as well as physical signs of muggy and poisonous moisture, etc. in the bodies of shrimp, thereby reducing rapidly the mortality rate of sick shrimps. In addition, the three-stone alexipharmic pulverization addresses symptoms as well as root causes and can remarkably improve the immunity of shrimp bodies.
US20090137542 Alpha-glucosidase inhibitors from fungal hydroxylation of tibolone and hydroxytibolones Sixteen new and one known metabolites were obtained by incubation of tibolone and hydroxytibolones with various fungi. Their structures were elucidated by means of a homo and heteronuclear 2D NMR and by HREI-MS techniques. The relative stereochemistry was deduced by 2D NOESY experiment. These metabolites have shown promising inhibitory activities against α-glucosidase enzyme. Seven metabolites exhibited potent inhibitory activity against the α-glucosidase enzyme and were thus found useful in the treatment of diabetes mellitus and other diseases related to the activity of α-glucosidase enzyme.
US20110021521 Fused heterocyclic compounds as ion channel modulators The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
CN102600252A Defervescence composition for enema of children The invention discloses a defervescence composition for enema of children, which is prepared from the following pharmacodynamic raw materials in a proportion: 10g of Chinese thorowax root, 15g of kudzuvine root, 5g of liquorice, 10g of baical skullcap root, 15g of Chinese peony, 15g of gypsum, 5g of cassia twig, 10g of perilla leaf, and 6g of Chinese rhubarb. The composition has the advantages of good curative effect, few adverse responses, easiness in acceptance of children and parents and simpleness in operation.
US20110287025 Combination therapy and method for assessing resistance to treatment The present invention relates to a method for determining a subject's resistance to treatment with 2,2-dimethyl-N—((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide by measuring the levels a biomarker or biomarkers present in a biological sample obtained from the subject, the biomarker being IL6 and/or IL8. The present invention also relates to a combination therapy for a patient suffering from a proliferative disorder comprising administering to the patient 2,2-Dimethyl-N—((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide and an anti-IL6 and/or an anti-IL8 agent.
WO2014106126A1 Scalp and/or hair treatment compositions and combinations Provided herein are sulfate free and/or sodium chloride free scalp and/or hair treatment compositions comprising corticosteroid, combinations containing these compositions, kits and methods, particularly for treating hair and/or treating and/or preventing itchy scalp.
WO2008105181A1 Pharmaceutical agent for prevention and/or treatment of lower urinary tract symptom Disclosed is a pharmaceutical agent for the prevention and/or treatment of lower urinary tract symptom such as frequent urination induced by the lower urinary tract disorder. The pharmaceutical agent comprises a retinoid such as 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2- naphthalenyl)carbamoyl]benzoate as an active ingredient.
WO2008115413A1 Aromatase inhibitors for the treatment of mastalgia The present invention relates to a method for treating, preventing or moderating mastalgia in a patient, which includes administering to the patient in need thereof a pharmaceutically effective amount of an aromatase inhibitor. The aromatase inhibitor, preferably letrozole, anastrozole or exemestane, may be used alone or in combination with danazol.
US20110190291 Prodrug and Fluoregenic Compositions and Methods for Using the Same Methods and compositions for treating disease caused by increased iron levels are disclosed Fluoregenic compounds and methods of using the same are also described.
CA2269217C New 1,7,7-trimethyl-bicyclo[2.2.1]heptane derivatives The new compound of Formula (I) and salts thereof possess valuable anxiolytic properties.
EP2364967A2 Process for preparation of rasagiline and salts thereof The present invention relates to an improved process for the preparation of Rasagiline or pharmaceutically acceptable salts thereof. The present invention also relates to Rasagiline salts, polymorphs thereof and process for preparation thereof.
CA2375364C Process for preparing 6-o-alkenyl-substituted erythromycin derivatives In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4"-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.
WO2009073192A3 Systems and methods for delivery of materials Systems and methods for delivering release materials, for example drugs and other bioactive materials. Crystalline polymeric systems, referred to as CYC carriers, are associated with the release materials, through chemical bonding or through physical association. The crystallinity of the CYC carriers results from the presence of crystallizable side chains, for example long chain n-alkyl moieties, which results in relatively low and sharp melting temperatures. One class of CYC carriers, referred to as CYSC polymers, have a majority of the crystallizable side chains pendant from the polymer backbone. Another class of CYC carriers, referred to as ECC polymers, have a majority of the crystallizable side chains attached to terminal units of the polymer backbone. The ECC polymers can for example be obtained by modification of PLGA polymers. The CYC carriers in another class of non-polymeric. Some CYC carriers, referred to as CYC assemblies, have enhanced crystallinity as a result of the physical association of crystallizable moieties which are present in different types of molecule, for example between a polymer containing crystallizable moieties and a monomer containing crystallizable moieties. For some uses, particularly the delivery of drugs, a bioerodable CYC carrier is preferably used.
US20120207816 Transdermally Absorbable Donepezil-Containing Preparation Provided is a donepezil-containing transdermal absorption formulation that can sustainably administer donepezil for a long period of time, and can provide both a rapid increase in the blood level of donepezil and donepezil sustained release properties. The donepezil-containing transdermal absorption formulation is a transdermal absorption formulation produced by dissolving donepezil, which is the active ingredient, in an adhesive patch base that contains a hydrophobic polymer and an absorption promoter. The absorption promoter is one kind or two or more kinds selected from lauryl alcohol, triethyl citrate, isopropyl myristate, cetyl lactate, oleyl alcohol, sorbitan monooleate, polyethylene glycol monostearate, lauromacrogol, N-methyl-2-pyrrolidone, and triacetin.
CN101756926A Ofloxacin slow-release tablet and preparation method thereof The invention aims at providing an ofloxacin slow-release tablet with higher medicine release stability and higher medicine application safety of the medicine. The invention is characterized in that the ofloxacin slow-release tablet is prepared from one or more than one ingredients of ofloxacin, slow release materials, expanding agents, filling agents, adhesive agents, gas generating agents, glidants, lubricating agents, wetting agents and filming materials. The ofloxacin slow-release tablet prepared by the invention has the characteristics of convenient medicine administration, persistent effect, stable curative effect, small toxic or side effect and the like.
US7547700 Such as (3-chloro-4-fluorophenyl)(4-fluoro-4-{[(5-hydoxypyridin-2-ylmethyl)amino]methyl}piperidin-1-yl)methanone; serotonin receptor agonists; for treating depression, pain, and substance abuse The invention relates to compounds of general formula (1) in which X and Y=a carbon with a bonded hydrogen atom (CH) or a nitrogen atom, A=a methyl, fluoromethyl, cyano, hydroxyl, methoxy group, or a chlorine or fluorine atom on condition that when A=methyl (CH3) and X and Y both=a carbon bonded to a hydrogen atom, then B=a chlorine atom, B=a chlorine or a fluorine atom, D=a hydrogen, chlorine, fluorine atom, or a cyano or trifluoromethyl group and E=a hydrogen, fluorine or chlorine atom.
US7704979 Materials and methods for the treatment or prevention of obesity The subject invention provides methods of inducing the loss of adipose tissue by providing a diet high in calcium. In one aspect of the invention, the calcium is provided in the form of dairy products. In yet another aspect of the invention, calcium is provided in the form of a dietary supplement, such as calcium carbonate, of vitamin supplements. Methods of suppressing [Ca2+]i levels in individuals are also provided. The subject invention also provides methods of stimulating lipolysis, inhibiting lipogenesis, and increasing the expression of white adipose tissue uncoupling protein 2 (UPC2). The subject invention also provides methods of increasing the core temperature of an individual.
CN103127130A Cefotaxime sodium pharmaceutical composition powder injection The invention provides a cefotaxime sodium pharmaceutical composition powder injection, relating to the field of a pharmaceutical preparation and a preparation method thereof. The invention mainly solves the problems of high dosage of single cefotaxime sodium and metronidazole preparation, poor treatment effect after combination, and great side effect in the prior art. The pharmaceutical composition comprises cefotaxime sodium and metronidazole lipid microspheres in a weight ratio of 100:3-100:9, wherein the weight of the metronidazole lipid microspheres is metered on the basis of on metronidazole; and when the pharmaceutical composition is prepared into a powder injection, the pH value of the water solution of the pharmaceutical composition is 4.5-6.5. The pharmaceutical composition powder injection provided by the invention has high curative effect, and can reduce the consumption of the metronidazole by more than 80%, thereby greatly relieving or avoiding the toxic and side effects of the metronidazole, especially digestive tract reactions, including nausea, vomit, inappetence, abdominal colic and neurotoxicity, and lowering the incidence rate of adverse reactions.
WO2013167909A1 Herpes simplex virus for the treatment of liver cancer An oncolytic herpes simplex virus is disclosed for use in a method of treating primary liver cancer.
US20070219118 Therapeutic methods for nucleic acid delivery vehicles It has been found that certain synthetic vectors and nucleic acid sequences that encode viral genomic sequences can, for example, be administered to a subject repeatedly as a vehicle for effectively delivering one or more therapeutic nucleic acid molecules or polypeptides to a cell or tissue. Accordingly, the disclosed nucleic acid delivery vehicles can be used, for instance, as part of a therapeutic regimen that involves an ongoing use of a therapeutic nucleic acid molecule or polypeptide.
US20070265213 Use of Docetaxel/Doxorubicin/Cyclophosphamide in Adjuvant Therapy The present invention relates to a new method of adjuvant therapy in the treatment of early breast cancer, comprising administering six cycles of docetaxel, doxorubicin and cyclophosphamide to a patient in need thereof, wherein said dosages have a marked therapeutic effect when compared to other adjuvant therapies.
WO2009085262A1 Method of treating cancer with immunomodulatory compounds and igg Provided herein relates to the field of cancer and its treatment by administering immunomodulatory compounds in combination with other compounds. In particular, a combination of an immunomodulatory compound and an antibody is provided.
US20110118300 Glucose metabolism modulating compounds The present invention provides, inter alia, dihydropyridone compounds and compositions, including analogs of a vesicular monoamine transporter type 2 (VMAT2) antagonist. The present invention also provides methods of using such compounds/analogs for modulating glucose levels, and/or preventing, treating, or ameliorating the effects of diabetes and hyper-glycemia.
US20110288144 Use of hdac inhibitors for the treatment of melanoma The invention relates to the use of an HDAC inhibitor, more specifically or a pharmaceutically acceptable salt thereof for the manufacture of pharmaceutical compositions for the treatment of melanoma; the use of an HDAC inhibitor or a pharmaceutically acceptable salt thereof in the treatment of melanoma; a method of treating warm-blooded animals including mammals, especially humans, suffering from melanoma by administering to a said animal in need of such treatment a dose effective against said disease of an HDAC inhibitor or a pharmaceutically acceptable salt thereof.
CN103721242A New application of pharmaceutical composition in prevention or treatment of osteoporosis The invention provides new application of a pharmaceutical composition. The pharmaceutical composition is composed of the following components in percentage by weight: 15-35% of glucosamine hydrochloride, 20-40% of biological calcium carbonate, 5-20% of rhizoma drynariae extracts, 1-5% of casein phosphopeptides, 10-20% of chondroitin sulfate, and 10-30% of epimedium extracts. The new application is that the pharmaceutical composition is used for preparing drugs or health-care products for preventing or treating osteoporosis.
WO2012099477A1 Biosurface engineering The invention relates to methods of localising biofunctional moieties (F) to surfaces and synthetic constructs of the general structure F-S-S' for use in such methods. F is the biofunctional moiety, S is a spacer covalently linking F to S', and S' is sterol. In particular, the invention relates to the preparation of biofunctional surfaces and surface modified biological structures including cells (kodecytes), enveloped viruses (kodevirions) and liposomes or virosomes (kodesomes).
US20090304819 Systemic Treatment of Pathological Conditions Resulting from Oxidative Stress and/or Redox Imbalance Alterations of redox homeostasis in mammals underlie a host of symptoms, syndromes and diseases, including AIDS and cancer, which can be successfully treated by administration to a mammal of therapeutically-effective amounts of sulfide compounds and/or thiosulfate compounds and/or thionite compounds and/or sulfite compounds and/or thionate compounds and/or any organic, inorganic or organometallic precursors thereof. The unique compositions of this invention contain one or more “active sulfur compounds” in combination with each other or with other therapeutic agents. The invention also encompasses the varying modes of administration of the therapeutic compounds. In particular, a novel method of combining active ingredient with wet cellulose is provided, which allows the wet cellulose to function as an enteric carrier.
US20090203729 Process for Producing High-Purity Prasugrel and Acid Addition Salt Thereof The present invention is directed to providing prasugrel hydrochloride or the like with a reduced content of OXTP. A method for producing prasugrel hydrochloride with a reduced content of OXTP, comprising dissolving free prasugrel containing OXTP in an inert solvent and adding hydrochloric acid optionally dropwise to the solution for reaction is also provided.
EP1876239A1 Degranulation inhibitor The present invention provides a screening method/screening kit for a mast cell degranulation inhibitor which is characterized by using (a) a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, its partial peptide, or a salt thereof and (b) a ligand capable of specifically binding to the protein; a mast cell degranulation inhibitor obtained by the screening; and so on.
US20110124706 SOCS3 Inhibition Promotes CNS Neuron Regeneration Regeneration of injured CNS neurons in a mammal in need thereof is promoted by delivering directly to the body of the injured CNS neurons, such as with an intracerebral or intraretinal cannula, an effective amount of a specific inhibitor of SOCS3.
US20090105257 Aminophenylcyclopropyl carboxylic acids and derivatives as agonists to gpr40 The present invention relates generally to novel therapeutic compounds and more particularly to novel compounds, their use as GPR40 agonists, processes for their manufacture, and intermediates useful in their preparation.
WO2008000079A1 Secreted protein acidic and rich in cysteine (sparc) as chemotherapeutic sensitizers The present invention relates to compositions and methods of use thereof for cancer therapy sensitization. Such compositions comprise functional fragments of the nucleotide and/or polypeptide sequences of a Secreted Protein Acidic and Rich in Cysteine (SPARC). The compositions can be used in combination with existing chemotherapeutic agents for treatment of cancers.
CN1329026C Pharmaceutical composition comprising (-)-secoisolariciresinol This invention relates to a pharmaceutical composition comprising an effective amount of (-)-Secoisolariciresinol together with or associated with an additive useful as an antioxidant; a process for isolating the (-)-Secoisolariciresinol from the plant Stereospermum Personatum and also relates to use of the active fraction (-)-Secoisolariciresinol as an antioxidant or free radical scavenger.
US20100015221 Orally rapid disintegrating tablet preparation comprising fat-soluble active ingredients The present invention provides an orally rapid disintegrating tablet preparation that contains a high dose of a fat-soluble active ingredient, that exhibits excellent disintegration characteristics in the oral cavity, and that can be produced by a dry tabletting method. The present invention also provides a method of producing an orally rapid disintegrating tablet preparation. The present invention discloses an orally rapid disintegrating tablet preparation that is obtained by tabletting a uniform mixture prepared by mixing saccharide alcohol, crystalline cellulose, and a lubricant with a granule that has been produced by the adsorption of a fat-soluble active ingredient on a porous material.
EP1923066A1 Composition comprising rooibos tea and conjugated linoleic acid (CLA) Composition (I) comprises red shrub tea and conjugated linoleic acid. - ACTIVITY : Antiallergic; Antiasthmatic; Antiinflammatory; Cardiant; Cerebroprotective; Vasotropic; Antiulcer; Gastrointestinal-Gen; Antidiabetic; Nootropic; Dermatological. - MECHANISM OF ACTION : None given.
WO2010101649A3 Sigma 1 receptor inhibition as a novel therapeutical approach against hepatitis c virus infection A method for treating or ameliorating the symptoms of a Hepatitis C virus infection comprising administering a Sigma 1 receptor binding compound or an interfering RNA is provided. Methods for identifying a compound that inhibits a Hepatitis C virus infection are also provided. The Sigma 1 receptor binding compound or interfering RNA is believed to act by reducing the susceptibility of uninfected human cells to infection by Hepatitis C virus, inhibiting viral spread in a cellular population.
WO2013188848A3 Antiviral compounds and methods of use Methods for treating enteroviral infections in cells are provided. Aspects of the methods include inhibiting the replication of enterovirus or replication of other virus and/or inhibiting cell death in a cell infected with enterovirus or other viruses.
US6984657 Indole derivatives as MCP-1 receptor antagonists A compound of Formula I, wherein: R1 is hydrogen, halo, methyl, ethyl or methoxy; R2 is hydrogen, halo, methyl, ethyl or methoxy; R3 is a halo group, lower alkyl, lower alkenyl, lower alkynyl, alkoxy, trifluoromethyl, nitro, cyano, trifluoromethoxy, C(O)R7, or S(O)nR7 where n is 0, 1 or 2 and R7 is an alkyl group; R4 is a halo, trifluoromethyl, methylthio, methoxy, trifluoromethoxy or lower alkyl, lower alkenyl or lower alkynyl or COR8 where R8 is lower alkyl; R6 is hydrogen, halo, lower alkyl, lower alkenyl, lower alkynyl or COR9 where R9 is lower alkyl; provided that when R1 is hydrogen, halo or methoxy, R2 is hydrogen, halo, methyl, ethyl or methoxy, R5 and R6 are both hydrogen, and one of R3 or R4 is not halo or trifluoromethyl; or a pharmaceutically acceptable salt or prodrug thereof. These compounds have useful activity for the treatment of inflammatory disease, specifically in antagonizing an MCP-1 mediated effect in a warm-blooded animal such as a human being.
CN102525923A Preparation method of carotenoid emulsion and microcapsules The invention discloses a preparation method of carotenoid emulsion and microcapsules. The method is characterized in that the electrostatic force interaction of emulsifier molecules on an emulsion interface is utilized, and a two-step homogenization method is applied to preparing carotenoid bilayer emulsion which can be further dried to prepare carotenoid microcapsules. The method disclosed by the invention is simple, convenient and feasible for preparation, the used emulsifier and microcapsule wall materials have favorable biocompatibility and can be biodegraded, and a material source range is wide; and the carotenoid emulsion and microcapsules have the characteristics of good physical and chemical stability, long shelf life and the like, the carotenoid loading capacity of the emulsion can reach 2%, and the carotenoid loading capacity of the microcapsules can reach 10%.
CN102516385A Nerve growth factor-paclitaxel conjugate, manufacturing method and uses thereof The invention relates to a nerve growth factor-paclitaxel conjugate. By using a nerve growth factor as a carrier, succinic acid is conjugated with paclitaxel to obtain the nerve growth factor-paclitaxel conjugate in which 1-6 paclitaxel molecules are connected onto one nerve growth factor. The nerve growth factor-paclitaxel conjugate provided by the invention is a white solid, and the solubility of the nerve growth factor-paclitaxel conjugate is increased by about 20 to 50 times compared with the solubility of a paclitaxel raw material. In the presence of the nerve growth factor, the nerve growth factor-paclitaxel conjugate plays a targeting role, can reduce damage to normal cells, effectively protects the safety of the lives of patients, and also improves the application of paclitaxel. Compared with the paclitaxel raw material, under the same concentration, the ability to inhibit tumor cells in vitro of the nerve growth factor-paclitaxel conjugate is stronger than that of the paclitaxel raw material.
WO2013192493A1 Nanoparticles of indirubin, derivatives thereof and methods of making and using same The disclosure provides nanoparticles of indirubin and methods of making and using these particles for the treatment of cancer, neurodegenerative disorders and inflammatory diseases. The effective average particle size of the nanoparticles is less than 2000 nm.
CN103040800A Application of gemfibrozil in preparation of anti-angiogenic medicaments The invention relates to application of gemfibrozil in preparation of anti-angiogenic medicaments. So far, reports on an anti-angiogenic activity of the gemfibrozil are not seen. The invention provides application of the gemfibrozil in preparation of anti-angiogenic medicaments, antineoplastic medicaments and exudative senile macular degeneration medicaments. An in vivo pharmacodynamic experiment carried out by a zebra fish angiogenesis model confirms that the vinpocetine can inhibit the zebra fish angiogenesis remarkably and the growth of the transplanted human cancer cells, and has a treatment effect on the exudative senile macular degeneration. Thus, the gemfibrozil can be applied to the preparation of the anti-angiogenic medicaments, the antineoplastic medicaments and the exudative senile macular degeneration medicaments.
CN102357081A Composite fat-soluble vitamin freeze-dried powder injection and preparation method thereof The invention discloses a preparation method of a composite fat-soluble vitamin freeze-dried powder injection. The preparation method comprises the following steps of: firstly, respectively adding fat-soluble vitamins A, E, K and D2 to polysorbate-80 to form two groups of micelle, and dissolving and mixing the two groups of micelle; secondly, adding water for injection, mixing with a mannitol aqueous solution, adding active carbon for adsorption, and regulating pH value; finally, filtering, bottling, freeze-drying, cover-pressing and sealing to obtain the finished freeze-dried powder injection product, wherein each 3.5 ml of freeze-dried powder injection solution contain 2970-3960 IU of vitamin A, 9-11 IU of vitamin E, 1135-180 ug of vitamin K, 2180-240 IU of vitamin D2, 50 mg of polysorbate-80, 120-180 mg of mannitol and the balance of water for injection. According to the invention, the composite fat-soluble vitamin freeze-dried powder injection and the preparation method thereof have the advantages of little auxiliary materials, simple preparation process, low production cost, safe and reliable quality and convenience for storage and transportation and the like.
EP1176146B1 Carbamoyl tetrahydropyridine derivatives Carbamoyl tetrahydropyridine derivatives represented by general formula (1) and being efficacious against CRF-related diseases; medicinally acceptable salts of the same; and intermediates for the preparation thereof, wherein R?1 and R2¿ are each independently hydrogen, C¿1?-C5 alkyl, or the like; Y?1-Y2 is (R4)C=C(R5), (R6¿)C=N, N=N, (R7)N-CO, or N=C(R?8); X1, X2 and X3¿ are each independently hydrogen, halogeno, or the like; R?3, R4, R5 and R6¿ are each independently hydrogen or alkyl; R7 is hydrogen, C¿1?-C5 alkyl, or the like; and R?8¿ is hydrogen or carbamoyl.
CA2163747C Novel 1-phenylalkanone 5-ht4 receptor ligands The present invention relates to novel 5-HT4 receptor ligands which are 1-(5-halo-4-aminophenyl) (C2-6)alkan-1-one derivatives in which the 5-halo-4-aminophenyl group is substituted at its 2-position with (C1-4)alkyloxy or phenyl(C1-4)alkyloxy and optionally substituted at its 3-position with (C1-4)alkyloxy or substituted at its 2- and 3-positions together with methylenedioxy or ethylenedioxy and the highest numbered carbon of the (C2-6)alkan-1-one is substituted with di(C1-4)alkylamino, morpholin-1-yl or pyrrolidin-1-yl or optionally substituted piperidin-1-yl, piperidin-4-yl, azacyclohept-1-yl, azabicyclo[2.2.1]hept-3-yl, azabicyclo[2.2.2]oct-3-yl or azabicyclo[3.2.2]non-3-yl; and the pharmaceutically acceptable salts, individual isomers and mixtures of isomers and methods of using and making such derivatives.
CN101884611B Method for preparing medicinal invert sugar by sugar hydrolysis The invention relates to a method for preparing medicinal invert sugar by sugar hydrolysis, which belongs to the technical field of preparation technology of medicaments and solves the problem that the invert sugar directly prepared by the sugar hydrolysis in the prior art cannot meet the medicinal standard. The method for preparing aqueous solution of medicinal invert sugar by directly hydrolyzing the sugar comprises the following steps of: adding 35 percent solution of concentrated hydrochloric acid into water for injection to adjust the pH value to a proper value; controlling a proper internal temperature and adding a proper amount of medicinal sugar to react for a certain time; and adding the injection water at the temperature of between 5 and 10 DEG C to rapidly reduce the temperature so as to obtain the aqueous solution of the medicinal invert sugar. The aqueous solution of the medicinal invert sugar prepared by the method can be used for preparing medicinal invert sugar injection and medicinal invert sugar electrolyte injection.
WO2014077570A1 Composition for preventing or treating inflammation The present invention relates to a composition comprising fimasartan, a pharmaceutically acceptable salt thereof, or a solvate or hydrate thereof, as an active ingredient, for preventing or treating inflammation or inflammatory diseases. The present invention can be used to prevent or treat blood diseases, arthritis, gastric ulcer, respiratory diseases, spondylitis, urethritis, cystitis, nephritis, allergic diseases, dermatomyositis, rhinitis, tonsillitis, acute pain, chronic pain, periodontitis, gingivitis, inflammatory bowel diseases, pancreatitis, RSV (respiratory syncitial virus) diseases, autoimmune diseases such as asthma, atopic dermatomyositis, Crohn's disease, rheumatic arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, and so forth.
US6849421 Nucleotide sequences coding enzymatic polypeptide for the use in the treatment of nervous system disorders Here we describe the molecular identification of a cDNA encoding a novel serine protease we have termed protease C-E. The deduced amino acid sequence, and it alignment with other well-characterized serine proteases indicates that it is a member of the S1 serine protease family. We have found that the protease C-E mRNA is expressed in pancreas, placenta, prostate, small intestine, stomach, spleen, fibroblasts and epidermis, as well as in certain regions of the brain i.e., cerebellum, cerebral cortex, pituitary and hippocampus. Enzymatically active protease C-E, as produced using the methodologies described herein, is amenable to further biochemical analyses for the identification of physiological substrates and specific modulators.
WO2010080730A2 Methods and materials for delivering bile acids This document relates to methods and materials for administering bile acid compounds to treat conditions associated with constipation. For example, formulations designed for the delayed-release of a bile acid compound (e.g., sodium chenodeoxycholate) to treat constipation are provided.
WO2004092170A3 Triazolotriazines and pyrazolotriazines useful as a2a adenosine receptor antagon ists The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkinson’s disease. In one embodiment, the invention features a compound of formula I: (I)
US20080287351 Nfkb Transcriptional Activity Inhibitory Agent and Anti-Inflammatory Agent and a Steroid Action Enhancing Agent It is intended to surely and effectively inhibit the transcriptional activity of NFκB and to obtain a more effective anti-inflammatory effect. Further, it is intended to obtain an equivalent effect even if the amount used of a steroid agent is reduced. An agent is characterized by containing MTI-II, especially a nucleic acid sequence of SEQ ID NO: 1, or a peptide of SEQ ID NO: 2. This MTI-II peptide is preferably a peptide containing at least an acidic amino acid domain (SEQ ID NO: 3). Further, a steroid agent such as triamcinolone acetonide is used concomitantly with MTI-II, especially the nucleic acid sequence of SEQ ID NO: 1 or the peptide of SEQ ID NO: 2.
CN102657872A Multifunctional graphene oxide/ polyamide-amine (PAMAM)/ diethylene triamine pentaacetic-gadolinium (DTPA-Gd)/ prostate stem cell antigen (PSCA) antibody material and preparation method and application thereof The invention discloses a multifunctional graphene oxide/ polyamide-amine (PAMAM)/ diethylene triamine pentaacetic-gadolinium (DTPA-Gd)/ prostate stem cell antigen (PSCA) antibody material. PAMAM dendrimers are covalently modified on nano graphene oxide flakes, and DTPA-Gd and PSCA antibodies are modified by using amino on the PAMAM dendrimers. The obtained material has very high biocompatibility and stability, can be used as a good T1 contrast medium, and has a good targeting property for prostatic cancer cells; and doxorubicin hydrochloride can be adsorbed to the graphene oxide/ PAMAM/ DTPA-Gd/ PSCA antibody material under coaction of phi-phi bonds, and the material is high in medicament loading rate and has an obvious targeting effect. The multifunctional graphene oxide/ PAMAM/ DTPA-Gd/ PSCA antibody material has targeting medicament loading and magnetic resonance imaging (MRI) functions, and has a very wide biological application prospect.
CN101401894A Compound formulation for medicament for diuresis and expelling stone The invention relates to a method for dispensing a medicine for promoting urination and expelling stones. 40 percent of talcum, 40 percent of white peony root, 10 percent of rhizoma anemarrhenae and 10 percent of phellodendron are adopted, pulverized, sifted by a 100-mesh sieve and are subjected to high-speed mixing, drying, pelletization and packaging to obtain the medicine for promoting urination and expelling stones. The medicine is used for treating urinary calculus and has the function of promoting urination and expelling stones.
WO2006097817A9 N- (n-sulfonylaminomethyl) cyclopropanecarboxamide derivatives useful for the treatment of pain This invention provides a compound of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compounds.
CN1880313A Novel heterocycle naphthoylimine and double-chain compound and its uses in tumour cell This invention relates to a naphthalene imide derivant and the application thereof. The said derivant is produced by adding a hetero ring to the aromatic ring of acridine or phenazine compound, structure indicated by formula(I). Compared to the current acridine or phenazine compounds, the DNA inlay ability of the said derivant is improved, and thereby it improves their antineoplastic activity, especially shows distinct suppression activity on the proliferation of tumour cells from various tissue sources like human lung carcinoma, gastric cancer, liver cancer and leukemia, and the effect shows a dose-effect relationship.
US20120196906 Substituted Imidazole Derivatives, Compositions, and Methods of Use as PTPase Inhibitors The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
CN201523733U Anti-plague spice-adorning product The utility model discloses an anti-plague spice-adorning product, which comprises a non-woven fabrics medicine bag and medicine powder which is sewed and evenly distributed in the non-woven fabrics medicine bag, wherein the non-woven fabrics medicine bag is externally provided with a rib fabric outer bag with the function of ventilation, and the rib fabric outer bag is ring-shaped. The anti-plague spice-adorning product has simple structure and convenient use, can be adorned with human bodies, can achieve the effects of flu prevention and plague avoidance, simultaneously can avoid difficulties caused by injecting and medicine taking, and has lower use cost.
US20090274651 Therapeutic agent for infections, and treatment method using the same (Problems) To provide a therapeutic agent for infections comprising granulysin as an active ingredient which has little side effect and no cytotoxicity and to which bacteria can hardly acquire resistance, and a treatment method using the same. (Means for Solving Problems) The present invention provides a therapeutic agent for infections comprising as active ingredient: 15K granulysin, a combination of 15K granulysin and 15K granulysin in vivo expression vector, a combination of 15K granulysin and at least one interleukin selected from IL-6, IL-23 or IL-27, a combination of 15K granulysin in vivo expression vector and at least one interleukin selected from IL-6, IL-23 or IL-27, or a combination of 15K granulysin in vivo expression vector and HSP65DNA and IL-12DNA in vivo expression vector, which enhances killing effects on bacteria and has less side effect, and to which bacteria can hardly acquire resistance, and a treatment method using the same.
WO2007064502A1 Forms of n-[(4-fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide The invention relates to forms of N-[(4-fluorophenyl)methyl]-4,6,7,9- tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2; 1 -c][l ,4]oxazine-2- carboxamide (Compound I) which is an HIV integrase inhibitor useful in the treatment of AIDS and HIV infection. Various inventive aspects of Compound I are disclosed.
WO2010142652A1 Imidazobenzazepine compounds for the treatment of central nervous system (cns) diseases This invention relates to novel novel imidazobenzazepine derivatives of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.
US20110098301 Pyrimidine Derivatives for Treatment of Hyperproliferative Disorders Pyrimidine derivatives of formula pharmaceutical compositions containing these compounds, and methods of using these compounds in treatment of hyperproliferative diseases such as cancer are disclosed and claimed.
US7435834 2-thia-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof The present invention relates to compounds of 2-thia-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-α(TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.
US20120289578 Use of rna interference for treating or reducing pain A use of a nucleic acid molecule mediating RNA interference for treating or reducing pain is disclosed. The nucleic acid molecule has a sequence selected from the group consisting of SEQ ID NO:1, SEQ ID NO:2, SEQ ID NO:3 and SEQ ID NO:4, and is used for effectively inhibiting expression of bradykinin B2 receptor, treating or reducing pain and preparing a pharmaceutical composition for reducing neuropathic pain.
US8853173 Synthetic glycolipid and use thereof A compound represented by the following formula (1): wherein R1 is an aldopyranose residue wherein the 6-hydroxyl group is optionally alkylated, R2 is a C1-26 hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom or a C1-26 hydrocarbon group optionally having substituent(s), R4 is a C1-21 hydrocarbon group optionally having substituent(s), X is an oxygen atom or —CH2—, and Y is —CH2—, —CH(OH)— or —CH═CH—, or a salt thereof is useful for the prophylaxis or treatment of cancer or infection, since it can preferentially induce production of IFN-γ of NKT cells.
US20090186056 Compositions and methods for preventing infection This invention relates to cholesterol-sequestering agents and methods of using cholesterol-sequestering agents to prevent infection. The compositions of the invention can be used to decontaminate skin and environmental surfaces that are contacted with microorganisms such as envelope viruses.
WO2013045652A1 Inhibition of microrna-134 for the treatment of seizure-related disorders and neurologic injuries A method for preventing or treating epilepsy or status epilepticus, or a brain-related disorder characterised by precipitation of seizures, in an individual, the method comprising the step of treating the individual with an agent capable of inhibiting the activity of miR-134 in the individual, wherein the agent is delivered to the brain of the individual.
WO2014048921A1 Combinations and uses thereof The present disclosure describes a pharmaceutical combination of an anti-CD38 antibody and melphalan.
CN102579626A Compound aged-vinegar dropping pill and preparation method thereof The invention belongs to the technical field of healthcare food, and discloses a compound aged-vinegar dropping pill and a preparation method thereof. The compound aged-vinegar dropping pill comprises ginkgo leaf extracts, panax notoginseng saponins or hawthorn leaf extracts, aged vinegar (aged vinegar starch) and basic substances. The prescription of the dropping pill disclosed by the invention is determined through a scientific screening test. Proved by the test, the compound aged-vinegar dropping pill disclosed by the invention has good healthcare effects, such as hypoxia resistance and an anti-lipidemic effect.
CN103585169A Pharmaceutical composition capable of increasing the content and the utilization degree of cyclic adenosine monophosphate in vivo and manufacturing method of the pharmaceutical composition The invention discloses an oral medicine or a health-care food, wherein the oral medicine or the health-care food which is capable of increasing the content and the utilization degree of cyclic adenosine monophosphate (cAMP) in vivo is manufactured by using panaxosides (Rg1+Rb1+Re), glycyrrhizic acid and jujube cAMP as the main components.
EP1782813A1 The combination of a serotonin reuptake inhibitor and a 5-HT2C antagonist, inverse agonist or partial agonist The present invention relates to the use of compounds and compositions of compounds having serotonin reuptake inhibiting activity and 5-HT2C antagonistic, partial agonistic or inverse agonistic activity for the for the treatment of depression and other affective disorders. The combined serotonin reuptake inhibiting effect and the 5-HT2C antagonistic, partial agonistic or inverse agonistic effect may reside within the same chemical compound or in two different chemical compounds.
CN102448958A Pyrimddinyl and 1,3,5-triazinyl benzimtoazole sulfonamides and their use in cancer therapy Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae (IA), (IB), and (IC), and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
CN101791299A Method for preparing potassium citrate sustained-release tablets The invention relates to a formula and a process for preparing potassium citrate sustained-release tablets, belonging to the technical field of the medicine. The potassium citrate sustained-release tablets are prepared by mixing pore-forming agent, filler, lubricant and coloring agent which are pharmaceutically acceptable to stearic acid or stearic acid derivative, ethyl cellulose, polyacrylic acid resin and glyceryl monostearate which are used as insoluble framework materials according to a certain proportion. The potassium citrate sustained-release tablets have attractive appearance and can release stably in various release medium and even for 6 months in the acceleration test at 40 DEG C.
CN101019914A Soft capsule containing lutein and its prepn The present invention discloses one kind of soft capsule containing lutein and its preparation process. The soft capsule has inclusion comprising lutein 62.4-109.2 weight portions, mountain mulberry fruit 3.12-9.36 weight portions, docosahexaenoic acid 156-218.4 weight portions, yeast astacin 6.24-21.84 weight portions, vitamin E 3.12-9.36 weight portions, vitamin B2 3.12 -9.36 weight portions and zinc gluconate3.12-9.36 weight portions. The soft capsule has the functions of protecting eyesight, regulating blood fat, reducing risk of heart diseases, etc.
EP2374788A1 Indanyl compounds Problems to be solved are to provide novel low-molecular compounds which exhibit calcium receptor antagonist activity, and which are highly safe and orally administrable. Means for solving the problems are the compounds having the Formula (I) or pharmaceutically acceptable salts thereof: [in the formula, each substituent is defined as follows. A: a single bond or the like; D: a single bond or the like; R2a and R2b: the same or different from each other, a hydrogen atom, a halogen atom, or the like; R3a and R3b : the same or different from each other, a hydrogen atom, a halogen atom, or the like; R4 and R5: the same or different from each other, a hydrogen atom, a halogen atom, or the like; R6: a methyl group, an ethyl group, or the like; m: an integer of 0 to 6, or the like; Z: a carboxy group or the like]
WO2006006082A3 Multi-ring compounds for regulating gut motility, food intake, and weight gain Multi-ring organic compounds that regulate gut motor activity, signal satiety, and reduce food intake in an individual are described Such compounds are useful to regulate food consumption and to treat conditions of excessive weight gam and obesity. These compounds are trichothecanes or trichothecenes of Formula I: wherein x is a single or double bond and R1 and R2 are, independently, selected from the group consisting of a branched or unbranched C1 to C6 alkyl group, a branched or unbranched C3 to C6 alkenyl group, a cyclic saturated C3-C6 ring, a monounsaturated C4-C6 ring, an optionally substituted aryl group, and a 5 or 6-membered heteroaromatic ring
CN103505470A Production method for povidone-iodine solution The invention discloses a production method for a povidone-iodine solution which belongs to the field of antiseptic disinfectants. The povidone-iodine solution is prepared from povidone-iodine, polyvinylpyrrolidone, a quaternary ammonium salt cation surfactant, a medicinal reinforcing agent and drinking water through batching, blending and dissolving, split charging and the like. The method has the following main advantages: general equipment is used, the method is simple, product quality is good, poisonous and harmful gas and liquid are not discharged, and the produced povidone-iodine solution has the characteristics of a wide spectrum, high efficiency, long-lasting action, no toxicity, no stimulation, no corrosion and the like, exerts a good killing effect on bacteria, viruses and fungi and can be directly smeared on the surface of a wound on the skin or diluted 500 to 1000 times and sprayed in an animal building in use.
CN103372004A Application of Chukrasone B in preparation of medicines for resisting human body fungi The invention relates to an application of Chukrasone B in the preparation of medicines for resisting human body fungi, and belongs to the field of medicines. The Chukrasone B has a very strong inhibition effect on trichophyton rubrum, microsporum lanosum or trichophyton tonsurans, therefore, the Chukrasone B can serve as a compound capable of resisting human body fungi and is expected to be applied in the preparation of related medicines. The application of the Chukrasone B in the preparation of the medicines for resisting the human body fungi is disclosed by the invention for the first time. As the skeleton type of the Chukrasone B belongs to a bran-new skeleton type and the Chukrasone B has unexpected strong inhibitory activity on human body fungi, the possibility that other compounds provide revelation does not exist. The Chukrasone B has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for preventing and treating the human body fungi infection.
WO2010105008A3 Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents for the treatment of hematopoietic malignancies Combinations of PDK inhibitor compounds having Formula (I) and chemotherapeutic agents, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for treating hematopoietic malignancies. Methods of using such combinations for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
EP1645634A2 Transgenic animal models for cardiac hypertrophy and uses thereof The present invention relates to the use of a composition inhibiting the activity of CaMKIV and modulating the activity of at least one gene or gene product that is expressed in cardiomyocytes in response to a hypertrophic signal for the manufacture of a medicament for the treatment of cardiac hypertrophy, decompensated cardiac hypertrophy, compound cardiac hypertrophy, dilated cardiac hypertrophy, and heart failure.
CA2557443A1 Enhanced activity of hiv vaccine using a second generation immunomodulatory oligonucleotide The invention relates to the therapeutic use of a second generation immunomodulatory oligonucleotide in combination with HIV-1 antigen or immunogen to enhance the ability to reduce the risk HIV infection and to control the progression of HIV infection to prevent AIDS Related Complex (ARC) and AIDS.
CA2470342C Ribavirin granulate for producing coated tablets The present invention relates to a method for the production of a ribavirin-containing granulate, comprising the production of a granulate solution, mixing of a binding agent with an isopropanol/water- or ethanol/water-mixture, stirring the granulate solution into a mixture of ribavirin-powder with a hydrophilic or swellable solid adjuvant, and sieving and drying the resulting granulate, which is characterised in that the portion of isopropanol or ethanol of the alcohol/water-mixture is between 65% to 85% by weight. Based on this granulate, a ribavirin-tablet can be produced that can be used for the treatment of diseases, such as HCV.
CA2132613C Method and compositions for enhancing white blood cell functioning on a mucosal or cutaneous surface The present invention relates to a method for enhancing white blood cell functioning and metabolism on a mucosal surface of a mammal. The present invention also relates to a method for treating or preventing a condition in a mammal caused by the presence of a disease-causing agent on a mucosal surface or a cutaneous surface wherein the disease-causing agent can be diminished by the actions of the white blood cells. The present invention yet also relates to a method for healing a wound of a mucosal or cutaneous surface. The present invention also relates to compositions for use in such methods.
CA2619799A1 Methods for evaluating and implementing prostate disease treatments Provide is a method for evaluating test agents as candidates for treating prostatic diseases, including benign prostatic hyperplasia (BPH) and androgen dependent and androgen independent prostate cancer. The method comprises providing a mouse comprising a human prostate primary xenograft, where the xenograft contains blood vessels that include human endothelial cells, initiating androgen deprivation in the mouse, administering to the mouse a test agent within a period of 1-7 days after initiating the androgen deprivation, and determining a reduction in human epithelial cells in the xenografts and/or a reduction in number of the endothelial cells or blood vessels in the xenograft. Also provided is a method for treating an individual for human prostate cancer or benign prostatic hyperplasia. The method comprises initiating androgen deprivation in the individual and administering to the individual an agent capable of inducing apoptosis of vascular endothelial cells within a period of 1-7 days of initiating androgen deprivation.
CN102091025A Anti-tumor injectable hydrogel as well as preparation method and application thereof The invention relates to an anti-tumor injectable hydrogel as well as a preparation method and application thereof. The anti-tumor injectable hydrogel comprises the following materials by mass percent: 5%-10% of polyethylene glycol block-polyacrylic acid diblock copolymers, 0.1%-5% of cis-platinum (II) anti-tumor drugs, 8%-14% of alpha-cyclodextrin and the balance of water. Other polymers can be further added to the anti-tumor injectable hydrogel to form an anti-tumor mixed injectable hydrogel. The anti-tumor injectable hydrogel and the anti-tumor mixed injectable hydrogel can be used as therapeutic drugs of tumors.
EP2189157A1 EYE DROP COMPRISING DIBENZO[b,e]OXEPIN DERIVATIVE The present invention provides an eye drop comprising: a dibenz[b,e]oxepine derivative or a salt thereof and a polyvalent weak acid, an acidic amino acid or an amide thereof, a basic amino acid or an amide thereof, or the salt thereof, and the like, for the purpose of providing an eye drop or a preparation for topical administration which enables the concentration of a dibenz[b,e]oxepin derivative or a salt thereof to be high; or an eye drop or a preparation for topical administration comprising the dibenz[b,e]oxepine derivative or the salt thereof and having an effective composition for treating allergic disturbance or inflammatory disorder of an eye or for treating allergic disturbance or inflammatory disorder of a nose.
US20120156228 Methods, Kits, and Compositions for Generating New Hair Follicles and Growing Hair The invention features methods, kits, and compositions for generating new hair follicles and growing hair on a subject.
US7816516 Reacting hydroxyalkyl starch (HAS) with the bioactive agent in a medium that includes water; drug-HAS conjugates for treating tumors, arrythmia, infectious diseases; bioavailability; nontoxic solvents; biodrug activity is not inactivated The invention relates to compounds, comprising a conjugate of hydroxyalkyl starch (HAS) and an active agent, whereby the hydroxyalkyl starch is either directly covalently bonded to the active agent, or by means of a linker. The invention further relates to methods for the production of a covalent HAS-active agent conjugate, whereby HAS and an active agent are reacted in a reaction medium, characterised in that the reaction medium is water or a mixture of water and an organic solvent, comprising at least 10 wt. % water.
US8075917 Composition for solubilization of paclitaxel and preparation method thereof The present invention relates to a paclitaxel composition and the preparation methods thereof to solubilize paclitaxel wherein said composition comprises 4 to 90% by weight of at least one selected from the monoglycerides, 0.01 to 90% by weight of at least one oil and 0.01 to 20% by weight of paclitaxel. Also the present invention relates to a paclitaxel composition including emulsifiers and the preparation methods thereof to solubilize paclitaxel wherein said composition comprises 4 to 90% by weight of at least one selected from the monoglycerides, 0.01 to 90% by weight of at least one emulsifier and 0.01 to 20% by weight of paclitaxel. The composition of the present invention is an effective paclitaxel delivery system since the composition solubilizes paclitaxel, does not form aggregates after being dispersed in water, adsorbs well on the intestinal wall, and therefore has high bioavailability.
WO2011011882A8 Hydroxy fatty acid compounds and uses thereof for disease treatment and diagnosis A compound of formula (I): wherein R represents a hydroxy substituted C24 - C40 straight chain aliphatic group containing at least one double bond in the carbon chain; and at least one carbon in the chain is substituted with a hydroxy group. Such compounds are useful for detecting inflammation, inflammatory disorders and cancer in a subject, and can also be used in therapeutic applications including treatment and/or prevention of these conditions. Pharmaceutical compositions, combinations and supplements, as well as methods of treatment using the described compounds are therefore also described.
CN103142640A Health care product containing vitamin K2 and having functions of preventing and treating brittle-bone disease The invention relates to a health care product containing vitamin K2 and having functions of preventing and treating brittle-bone disease. According to the technical scheme, the health care product comprises 0.04-0.1 part of vitamin K2, 2-5 parts of calcium, 10-80 parts of pectic acid oligosaccharides, 1*10<-7>-6*10<-7> parts of vitamin D, and 5-20 parts of polypeptide, as well as auxiliary materials. The health care product is simply produced, and has the functions of efficiently preventing and treating the brittle-bone disease.
WO2011143872A9 Crystal form of (s)-4-hydroxy-2-oxo-1-pyrrolidine acetamide, preparation method and use thereof Crystal form I of (S)-oxiracetam and preparation method thereof are disclosed. The preparation method comprises the steps of preparing the crude product and crystallization, wherein acetone and water are used as solvents in the crystallization step. The use of the crystal form I of (S)-oxiracetam in preparing the medicine for preventing and treating memory dysfunction is also disclosed.
US20120014974 Methods of modulating cell death based on the bit1/aes regulatory pathway The present invention provides a method of identifying an effective agent that alters the association of a Bit1 polypeptide with an AES polypeptide. The method is practiced by contacting a Bit1 polypeptide, or active fragment thereof, and an AES polypeptide, or active fragment thereof, with an agent under conditions that allow the Bit1 polypeptide or active fragment thereof to associate with the AES polypeptide or active fragment thereof; and detecting an altered association of the Bit1 polypeptide or active fragment thereof and the AES polypeptide or active fragment thereof, where an altered association indicates that the agent is an effective agent that alters the association of a Bit1 polypeptide with an AES polypeptide. Such an effective agent can modulate apoptosis and can be a useful therapeutic agent.
WO2014002059A1 CRYSTALLINE FORMS OF 1-(2-((1R,3S,5R)-3-(((R)-1-(3-chloro-2-fluorophenyl)ethyl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-1Hpyrazolo[3,4-c]pyridine-3-carboxamide Crystalline forms of 11-(2-((1R,3S,5R)-3-(((R)-1-(3-chloro-2-fluorophenyl)ethyl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-1H- pyrazolo[3,4-c]pyridine-3-carboxamide. 1-(2-((1R,3S,5R)-3-(((R)-1-(3-chloro-2-fluorophenyl)ethyl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-1H- pyrazolo[3,4-c]pyridine-3-carboxamide is useful in treating a disorder or a disease in a subject mediated by complement activation, in particular mediated by activation of the complement alternative pathway.
CN1806822A Heat-clearing wetness-eliminating liver-dredging calculus removal liquid The invention discloses a heat-clearing wetness-eliminating liver-dredging calculus removal liquid, which is prepared from gentian root 10g, isatic root 60g, oriental wormwood 30g, Bupleurum root 20g, dandelion 30g, prepared magnolia obavata 12g, yellow-corktree bark 18g, baikal skullcap root 18g, glauber-salt and liquorice 18g, rhubarb horsetails 18g, burred tuber 10g and white peony root 20g through water grilling.
CN101317837B Effective component of rabdosia, preparation method and application thereof The present invention provides an effective component of rabdosia, which mainly comprises compound A, Coetsoidin F and compound B, and Coetsoidin C; wherein, the content of the compound A is between 70 to 90 percent, and that of the compound B ranges from 5 to 20 percent. The medicinal materials are heated, abstracted, condensed, separated by silicagel column, eluted, condensed and dried with eluent. Then the medicinal materials are separated by a liquid chromatography; subsequently, the solution is collected, and the active component is obtained after the solution is condensed and dried. Therabdosia provided by the present invention can be applied to the preparation of tumour cure and prevention medicine. The method of the present invention is reasonable. The effective ingredient can bequickly and accurately obtained. The quality of the medicine can be easily controlled in production.
WO2014058071A1 Cyclopropanamine compound and use thereof The present invention provides a compound that: has a lysine-specific demethylase-1-inhibiting effect; and provides utility as a drug for preventing or treating schizophrenia, Alzheimer's disease, Parkinson's disease, and Huntington chorea. The present invention pertains to a compound expressed by formula (1) or salt thereof (where (A) represents a hydrocarbon group optionally having a substitution group or a heterocyclic group optionally having a substitution group; (B) represents a benzene ring optionally having a substitution group; (R1), (R2), and (R3) independently represent a hydrogen, a hydrocarbon group optionally having a substitution group, or a heterocyclic ring group optionally having a substitution group; (A) and (R1) can be bonded together to form, with an adjacent nitrogen atom, a cyclic group optionally having a substitution group; and (R2) and (R3) can be bonded together to form, with an adjacent hydrogen atom, a cyclic group optionally having a substitution group).
US20080089859 Administration of sleep restorative agents The present invention provides methods and compositions for increasing the efficacy of a therapeutic agent administered to a subject. A steep restorative agent is co-administered to the subject along with the therapeutic agent, whereby the efficacy of the therapeutic agent is increased.
US7157582 For example, 3S,4aR,6S,8aR Ethyl 6-(((5S)-5-(Ethoxycarbonyl)-3-oxopyrrolidinyl) methyl)-2-methoxycarbonyl-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylate; for treating or preventing migraine The present invention provides a method of treating or preventing migraine comprising administering to a patient in need thereof an effective amount of a selective iGluR5 receptor antagonist. The present invention further provides novel compounds functional as selective iGluR5 receptor antagonists as well as compositions and formulations comprising said selective iGluR5 receptor antagonists.
CN102060764A Tetrahydroisoquinoline derivative, preparation method and application thereof The invention relates to a novel tetrahydroisoquinoline derivative, i.e. a compound in a general formula (I) and a pharmaceutically acceptable salt thereof. The invention also provides application of the novel tetrahydroisoquinoline derivative, in particular application to inhibiting multidrug resistance and improving the treatment effect of antitumor drugs.
US20110230557 Polyunsaturated fatty acid and diol ester as an anti-acne agent The present invention relates to compounds of the following formula (I): where n is an integer between 1 and 15, m is 0, 1, 2 or 3, and R is the hydrocarbon chain of a polyunsaturated fatty acid selected from among omega 3 and omega 6, as well as to pharmaceutical or cosmetic compositions containing same, to a method for preparing and using same, in particular for treating acne and seborrhoeic dermatitis.
WO2013091053A1 Polymer composition containing natural bioactive principles for use in pharmaceutical and cosmetic formulations The present invention relates to a polymer composition containing natural bioactive principles, in particular propolis extract. The present composition is of value because it exhibits antimicrobial (antibacterial, antifungal, antiviral and antiprotozoal), wound healing, anti-inflammatory, antioxidising and moisturising properties. The composition according to the present invention can be used in pharmaceutical and cosmetic formulations, thus being useful for odontological treatments (of caries, gingivitis, periodontitis, bad breath, aphthae, oral stomatitis) and for the treatment of affections of the skin and mucous membranes. The present composition also contains biocompatible and biodegradable polymers that allow controlled release of the active principles. For this purpose, the product can be provided in the form of different formulations: spray, mouthwash, toothpaste, oral-base cream, lotions, creams, gels, inter alia.
US20090082318 Deuterium-enriched mometasone The present application describes deuterium-enriched mometasone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US7175833 Glass composition A glass composition having the general empirical formula given below, expressed in weight percent of the element: P: 16–24, F: 5–30, O: 20–40 and at least one of Na, K, Li or Al in an amount up to a total of 40 wt. % and optionally, up to 5 wt. % of boron and/or silicon. The composition may be used for the treatment and/or prevention of dental caries by providing a slow fluoride releasing device that may be attached to a tooth to release fluoride into the saliva or an individual.
CN103619814A Novel amino-pyrroline derivatives, and use thereof in the prevention and/or treatment of metabolic syndrome The invention relates to novel amino-pyrroline derivatives, the pharmacologically acceptable salts thereof and the use of same in the prevention and/or treatment of metabolic syndrome.
US8703199 Pharmaceutical compositions of adsorbates of amorphous drug Pharmaceutical compositions comprise a low-solubility drug adsorbed onto a high surface area substrate to form an adsorbate. The compositions in some embodiments include a concentration-enhancing polymer.
CN101342299B Medicament for preventing and controlling white diarrhea disease The present invention discloses a medicine which is used for preventing and treating pullorum. The medicine comprises the ingredients of the following weight portions: 5 to 20 portions of Chinese pulsatilla, 5 to 20 portions of cortex moutan, 5 to 20 portions of bark of Chinese ash, 5 to 20 portions of purslane, 5 to 20 portions of myrobalan, 3 to 12 portions of radix geutianae, 3 to 12 portions of corktree, 3 to 12 portions of realgar, 3 to 12 portions of ageratum, 2 to 6 portions of garlic, 2 to 6 portions of banksian rose, 2 to 6 portions of rhubarb, 2 to 6 portions of talc and 2 to 6 portions of licorice. The herbs are insolated (excepting that the fresh garlic can be used), weighed, crushed, filtered by a sieve with 60 to 80 meshes, and mixed well, so as to prepare the medicine. Whenin clinical use, the medicine is dipped for 30 to 60 minutes in boiling water, so that the effective ingredients can be fully dissolved and separated to facilitate the absorption in the body of the sick chicken. Simultaneously, a small amount of sugar and Vc are added to improve the medicinal effects. The medicine has high cure rate, no adverse reaction, no drug residues in the body, and nearly no drug resistance. The production of the medicine has the advantages of easily acquirable raw materials, simple preparation, convenient use, and capability of wide promotion and application in the chicken breeding industry.
CN1562025A Cinrofloxacin eye preparation formula and its using method An ophthalmic medicine for cinrofloxacin is prepared from purified water, cinrofloxacin and isomolecular copolymer and/or homomolecular copolymer. It has less or no irritation to eyes.
US20090214536 CACNA1E in Cancer Diagnosis, Detection and Treatment This invention is in the field of cancer-related genes. Specifically it relates to methods for detecting cancer or the likelihood of developing cancer based on the presence or absence of the CACNA1E gene or proteins encoded by this gene. The invention also provides methods and molecules for upregulating or downregulating the CACNA1E gene.
US7264799 Administering to patient before or simultaneously with surgery at least one heparinase enzyme, wherein heparinase enzyme decreases localized inflammatory response in the tissue of the patient Heparinase enzymes can be used as a medical treatment to reduce localized inflammatory responses. Treatment of activated endothelium with heparinase inhibits leukocyte rolling, adhesion and extravasation. Most of the heparin and heparan sulfate on endothelial cell surfaces and in basement membranes is degraded by exposure to heparinase. In addition, immobilized chemokines, which are attached to heparin/heparan sulfate on activated endothelium are solubilized by heparinase digestion. Heparinase can be infused into the vascular system to inhibit accumulation of leukocytes in inflamed tissue and decrease damage resulting from localized inflammations. Targeting of heparinase to activated endothelium can be accomplished through localized administration and/or use of genetically engineered heparinase containing endothelium ligand-binding domains.
WO2008038053A1 Ion channel modulators & uses thereof Compounds of general formula (1) and pharmacologically acceptable salts and prodrugs thereof: Formula(1) wherein A and B are CH2 or CH2CH2, R1 is hydrogen, alkyl, cycloalkyl, aryl, aralkyl or heteroaralkyl, R2, R3 and R4 are selected from hydrogen, alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl or cyano; X is R5CO, R5SO2, R5R7NCO, R5R7NSO2, R5SO2NR7CO or CO2R8, Y is R6CO, R6SO2, R6R7NCO, R6R7NSO2, R6SO2NR7CO or CO2R8, R5 and R6 are hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl, R7 is hydrogen, alkyl, aryl or aralkyl, and R8 is alkyl, aryl, aralkyl, alkoxyalkyl, heteroaryl or heteroarylalkyl, are of use in the prophylaxis or treatment of diseases and conditions in which Kv1.x channels are involved, such as lower urinary tract disorders, cardiovascular diseases and pain.
CN102836185A Rodgersia sambucifolia hemsl medicinal composition with good stability and high bioavailability as well as preparation method and application The invention discloses a rodgersia sambucifolia hemsl medicinal composition with good stability and high bioavailability as well as a preparation method and an application of the medicinal composition. The composition provided by the invention comprises 1.5 to 5.0% by weight of rodgersia sambucifolia hemsl extract, 5.0 to 24.0% by weight of flavoring agent and the balance of bentonite. The method provided by the invention comprises the processes of active component extracting, ingredient processing and mixing; the active component extracting means grinding the rodgersia sambucifolia hemsl into coarse powder, extracting with ethanol, concentrating to obtain a paste, adjusting the pH value, filtrating and concentrating to obtain a thick paste, diluting, decoloring, filtrating and concentrating to obtain a concentrated thick paste, standing, filtrating the precipitate, and drying to obtain a rodgersia sambucifolia hemsl active component extract; crushing and screening the bentonite; and mixing a main material and the adjuvants to obtain a target composition. According to the invention, the rodgersia sambucifolia hemsl extract is taken as an active component of the medicinal composition, and the formula is reasonably arranged to completely give full play to the effect of the adjuvants on improving the physical and chemical property of a medicinal preparation and the gastrointestinal absorption capacity of the human bodies, so that the stability and the bioavailability of the preparation are improved, the taste is improved, and the crowds with fear of sugars suitable for the composition can be expanded.
CN101318933B Isoquinolinium compounds with antithrombotic activity, preparation method and application thereof The invention discloses compounds with anti-thrombus activity shown in a formula I, a preparation method thereof and an application of the compounds as antithrombotic agents. A rat thrombus model is adopted to evaluate the anti-thrombus activity of the compounds shown in the formula I. Experiment results show that: the compounds shown in the formula I have excellent anti-thrombus activity, and can be used as the antithrombotic agent clinically.
US20110150984 Methods of increasing the bioavailability and/or cellular update of drugs This invention pertains to methods of increasing the bioavailability and/or cellular uptake of an amphiphilic drug when administered parenterally, which method comprises the step of parenterally co-administering the drug with a short-chain sphingolipid as described herein.
CN1843347A 3-0- EGCG and ECG for resisting influenza virus The invention discloses a preparation using EGCG and ECG as effective constituents against influenza viruses, and the routes of administration include nasal cavity administration or oral cavity spraying administration.
US20090018150 5-Ht2b Receptor Antagonists Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT2B receptor.
US7547698 Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-coadesaturase (SCD) Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a compound of formula (I): where x, y, J, K, L, M, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
US20110178123 Nonpeptide hiv-1 protease inhibitors Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
CN102302747A Production formula and preparation method of quick-acting chilblain ointment The invention discloses a production formula and preparation method of a quick-acting chilblain ointment. The formula of the quick-acting chilblain ointment is prepared from the following components in parts by weight: 10-15 parts of monkshood, 10-15 parts of dried ginger, 5-10 parts of cinnamon, 5-10 parts of angelica, 10-20 parts of hemlock parsley, 10-15 parts of safflower, 5-10 parts of asarum, 3-10 parts of borneol and 300-500 parts of lard. In the medicines of the formula, the angelica, hemlock parsley and safflower have the function of activating blood circulation to dissipate blood stasis; the monkshood and dried ginger have the miraculous functions of warming the channels and stopping bleeding; the cinnamon, asarum and borneol have the functions of relieving exterior syndrome, dispelling cold, inhibiting inflammations and relieving pains; and the lard has the effects of moisturizing the dry skin, and helping the medicines enter the subcutaneous tissues of the human body. Thus, the chilblain ointment has the effects of relieving exterior syndrome, dispelling cold, activating blood circulation to dissipate blood stasis, relieving inflammatory pains, promoting circulation of qi, promoting the subsidence of swelling, warming the channels, stopping bleeding and moisturizing the dry skin, and has the advantages of high chilblain treatment speed and no relapse.
WO2009102808A2 Doxorubicin adjuvants to reduce toxicity and methods for using the same Methods are provided for using doxorubicin active agents in which reduced host toxicity is observed. Aspects of the methods including administering to a subject an effective amount of a doxorubicin active agent in conjunction with a doxorubicin toxicity-reducing adjuvant, e.g., a nitrone compound, or a nitrone compound in combination with a bisdioxopiperazine compound. Also provided are compositions for use in practicing the subject methods. The methods and compositions find use in a variety of different applications, including in the treatment of a variety of different disease conditions.
WO2004110344A3 New azetidine compounds The present invention relates to a compound of the general formula (I) wherein Het is an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring having at least one nitrogen atom; R1 is hydrogen, hydroxy, C1-C4 alkyl, C3-C4 cycloalkyl, C2-C4 alkenyl or C2-C4 alkynyl; R2 and R3 is each and independently selected from hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, C2-C4 alkenyl, C2-C4 alkynyl, C1-C4 alkoxy, halogen and cyano, provided that R2 and R3 may not both be hydrogen; R4 is C1-C4 alkyl, C3-C4 cycloalkyl, C2-C4 alkenyl or C2-C4 alkynyl; Ar is an optionally substituted aromatic ring system selected from pyridinyl; 1-naphthyl; 5,6,7,8-tetrahydro-1-naphthyl; quinolinyl; 2,3-dihydro-1,4-benzodioxinyl; 1,3-benzodioxolyl; 5,6,7,8-tetrahydroquinolinyl; 5,6,7,8-tetrahydroisoquinolinyl; 5,6,7,8-tetrahydroquinazolin-4-yl; 1-benzo[b]thiophen-7-yl; 1-benzo[b]thiophen-4-yl; 1-benzo[b]thiophen-3-yl; isoquinolinyl; quinazolinyl; and indan-4-yl; or Ar is substituted phenyl; or an enantiomer thereof or any salt thereof; to a pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of compounds of formula I and to new intermediates used in the preparation thereof.
EP1061803B1 Compositions of eprosartan This invention relates to a novel composition comprising eprosartan, or a salt, solvate, or hydrate thereof, in particulate form, a process for its production and methods of using the composition to block angiotensin II receptors and to treat hypertension, congestive heart failure and renal failure.
WO2014078645A1 Heterocyclic glutaminase inhibitors Disclosed herein are heterocyclic compounds containing thiadiazole and/or pyridazine rings, as well as pharmaceutical preparations thereof. The compounds herein are further made known to be useful as glutaminase inhibitors with potential uses in treating cancer, immunological and neurological diseases.
WO2007131689A3 Pharmaceutical combinations comprising a mtor inhibitor and a raf kinase inhibitor A pharmaceutical combination comprising an mTOR inhibitor and a Raf kinase inhibitor and its use.
WO2007047724A2 Compositions for lowering serum cholesterol and/or triglycerides The invention is directed to methods for treating disorders associated with hyperlipidemia in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, BMS-201038 and implitapide) and a fibrate (for example, fenofibrate). Co-administration of the MTP inhibitor with the fibrate produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit.
CN101716232B Quality control method of throat clearing dropping pill The invention relates to a quality control method of an HPLC finger-print of a throat clearing dropping pill. The method comprises the steps of the measurements of a high-polar finger-print taking gallic acid as a reference and a low-polar finger-print taking indigo blue as a reference, wherein the chromatographic column of the high-polar finger-print is Diamonsil C18 (4.6*250mm, 5 microns), gradient elution is adopted, a mobile phase A is acetonitrile, B is 0.1 percent phosphoric acid, the detection wavelength is 165nm, the column temperature is 25 DEG C, and the flowing speed is 1.0mL/min; the chromatographic column of the low-polar finger-print is Diamonsil C18 (4.6*250mm, 5 microns), the gradient elution is adopted, a mobile phase A is methanol, B is 0.1 percent phosphoric acid, the detection wavelength is 185nm, the column temperature is 30 DEG C, and the flowing speed is 1.0mL/min. By adopting the measuring method, the internal quality of the throat clearing dropping pill can be effectively controlled, and the method has the characteristics of high precision, stability, repetitiveness and guarantee of the stability and consistence of product quality, thereby guaranteeing the safety and effectiveness of a product.
US20070203206 2-Pyrrolidone Derivatives And Use Thereof As Factor Xa Inhibitors A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof.
WO2012034194A1 Method for mobilizing stem and/or progenitor cells The present disclosure relates to methods for mobilizing stem and/or progenitor cells which are VLA-4 positive to the peripheral blood of a subject or from a tissue. The method comprises administering to the subject or tissue an effective amount of an antisense compound to VLA-4.
CN101606987A Chinese veterinary medicament for preventing and treating animal viral disease The invention discloses a Chinese veterinary medicament for preventing and treating animal viral disease, which is characterized by comprising the following components in portion by weight: 80 to 100 portions of lobedfruit schizocapsa rhizome, 1 to 5 portions of propolis, 5 to 10 portions of moroxydine hydrochloride and 240 to 300 portions of starch. The Chinese veterinary medicament has the advantages of virus resistance, improvement of the immunity of organisms and no toxic and side effect, and avoids the occurrence of residual of a veterinary medicament and social effects of pollution.
CN103251580A Application of ampelopsin in preparation of vascular endothelial cell protection health food or drugs The present invention discloses an application of ampelopsin in preparation of vascular endothelial cell protection health food or drugs, wherein purified ampelopsin or an unpurified ampelopsin-containing extract can be adopted to prepare a pharmaceutically acceptable oral formulation, a pharmaceutically acceptable injection formulation or a pharmaceutically acceptable external application formulation, and the ampelopsin provides a vascular endothelial cell protection function through lipid peroxidation reduction, oxidative damage resistance and other effects so as to prevent and treat cardiovascular and cerebrovascular diseases caused by vascular endothelial cell damage, wherein the diseases comprise atherosclerosis, high blood pressure, heart and cerebral thrombosis, and the like.
WO2005016359A1 Method of promoting remyelination Methods and compositions for promoting the functional recovery and promoting remyelination of the nervous system are provided. The method involves administering an effective amount of a purine nucleoside to an animal in need thereof.
US7288280 Complete feed for fish larvae and method for preparing same The invention concerns a complete feed composition for fish larvae, characterized in that it has a phospholipid content not less than 8.5 wt. % of dry matter of the feed.
CN101502496B Method for preparing norfloxacin capsule The invention relates to a method for preparing norfloxacin capsules, which comprises the following steps: (1) evenly stirring norfloxacin and beta-cyclodextrin by the substance ratio of norfloxacin to Beta-cyclodextrin being 1:1, then, adding water and evenly grinding the mixture into paste for 6 to 10 hours at the temperature of 20 to 35 DEG C until the norfloxacin/Beta-cyclodextrin inclusion compound is formed; (2) tiling and drying the inclusion compound at the temperature of 45 to 60 DEG C; (3) pulverizing the dried inclusion compound, granulating the ground medicine through a 80-mesh sieve and drying at the temperature of 45 to 60 DEG C until the water content is lower than 9%; and (4) measuring the norfloxacin content of the granules, converting and filling a No.0 empty capsule with the granules to ensure that each granule contains 0.1g of norfloxacin, and finally packaging to obtain the norfloxacin capsules. The product of the invention has good water-solubility and improves the bioavailability and the stability.
WO2011114160A1 Anagrelide derivatives (imidazo [2, 1-b] quinazolin - 2 - ones ) as pde iii inhibitors useful as antithrombotic agents This invention relates to the discovery of 5-substituted analogues of the selective platelet lowering agent anagrelide, which are extremely potent inhibitors of phosphodiesterase III (PDE III). The compounds are potentially useful agents for the treatment of conditions in which the inhibition of PDE III in beneficial. Formula (I): wherein: R1 is independently selected form C1-6 alkyl or C1-6haloalkyl; R2 is selected from hydrogen, C1-6alkyl or C1-6haloalkyl; and X1 and X2 are each independently halo.
US20100184774 Methods of treatment This invention relates to a method of treating a disease state selected from: Alzheimer's disease, Down's syndrome, mental retardation, memory defects, memory loss, pancreatic cancer, bone resorption disease, osteoporosis, sickle cell anemia, chronic kidney disease, diabetes, depression, and subsets of depression including: alcoholism, anxiety, obsessive compulsive disorder, panic disorder, chronic pain, obesity, senile dementia, migraine, bulimia, anorexia, social phobia, pre-menstrual syndrome (PMS), adolescent depression, trichotillomania, dysthymia and substance abuse, in a mammal in need thereof, including a human, which comprises administering to such mammal a therapeutically effective amount of a selected substituted thiazol compound. The invention also relates to a method of enhancing cognition in a mammal in need thereof which comprises administering to such mammal a therapeutically effective amount of a selected substituted thiazol compound.
US8313769 Rapidly disintegrating dosage form for releasing active ingredients in the oral cavity or in body cavities A dosage form which is, in particular, sheet-like and rapidly disintegrating or soluble in an aqueous environment for rapid release of active ingredients in the oral cavity, in body orifices or in body cavities, where the dosage form comprises a matrix which comprises one or more water -soluble polymers as base substances, and comprises at least one active ingredient, is characterized in that the dosage form is provided with spaces or cavities which are present in the polymeric matrix and whose contents differ in terms of the state of aggregation from the matrix.
CN102532016A 5-aminoquinoline-2(1H) ketone compound and synthetic method and application thereof The invention discloses a novel 5-aminoquinoline-2(1H) ketone compound and a synthetic method and application thereof. A structure of the kind of compound is shown as the general formula I, (molecular formula) I, AR of (molecular formula) or (molecular formula). R1, R2 and R3 are hydrogen, halogen, methoxy group, methyl, nitro or acetoxyl group, R4 is hydrogen or acetyl, and X is oxygen or sulfur. A bioactivity test demonstrates that the 5-aminoquinoline-2(1H) ketone compound serves as an antimicrobial agent, is good in antimicrobial agent, and can be used for preparing drugs of etiology-resistant microorganism.
US20100216798 Fused heterocycles as lck inhibitors There is provided fused heterocycles of imidazopyridazine or pyrazolopyrimidine derivative represented by the formula (I), which have excellent Lck inhibitory activity and are useful for a medicament particularly an immunosuppressive agent. [wherein one of Y and Z is C atom, and the other is N atom; —X— is —N(R1)— or the like, —R1 represents hydrogen or the like, -A- represents bond or the like, —R2 is cycloalkyl, aryl or the like, -E- is bond or the like, —R3 is aryl, aromatic heterocycle or the like, —R4, —R5 and —R6 are the same or different, each being hydrogen or the like.]
WO2012052948A1 Pyridine- 2- derivatives as smoothened receptor modulators The present application relates to compounds of Formula (I), and Formula (II), or pharmaceutically acceptable salt thereof, wherein A, X, Y, Z, e, f, R1, R2, R3, R4, R5, R5b, R6, R7, R8, R9, R10, R11,R20, R21, R22 and R23 are defined herein. These novel pyridine derivatives that are useful in therapy, in particular for treating diseases or conditions mediated by Smo, including the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to methods of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
EP2646421A1 7-nitro-5-phenyl-1-(pyrrolidin-1-ylmethyl)-1h-benzo[e][1,4]diazepin-2(3h)-one and other benzodiazepine derivatives The present invention describes compounds of formula (I), and in particular the 7- nitro-5-phenyl-1 -(pyrrolidin-1 -ylmethyl)-1 H-benzo[e][1,4]diazepin-2(3H)-one compound and their pharmaceuticall acceptable salts. The compounds of the invention are useful for medical use, particularly as active ingredient potentially useful for the treatment of cerebral ischemia and other disease characterized by deregulation of sodium and calcium homeostasis.
CN103193771A New use of drug of chain amide CCR5 (chemokine receptor) receptor antagonist The invention discloses a new use of a drug of a chain amide CCR5 (chemokine receptor) receptor antagonist. The new use provided by the method is the chain amide CCR5 inhibitor or an application of pharmaceutically acceptable salt in the preparation of a spermicidal drug. The structure formula of the chain amide CCR5 inhibitor is shown in formula I. An inactivating sperm in vitro test proves that the series of compounds have strong sperm killing activity; the EC50 value of the compound with the strongest activity achieves 1.5mg/ml; and the chain amide CCR5 inhibitor can develop into a preparation for in vitro contraception, or a multifunctional external preparation for resisting aids and contraception.
WO2010037172A1 Antioxidant compounds and methods of their use The invention relates to antioxidant substituted isoindoline nitroxide compounds and their use in methods of treating or preventing diseases or disorders related to oxidative stress, methods of reducing oxidative stress and methods of protecting a subject from oxidative stress upon exposure to ionising radiation. Pharmaceutical compositions comprising the antioxidant compounds are also described.
CN101518527A Use of scutellarin in preventing or treating hepatofibrosis and method for preparing micropill thereof The invention relates to the use of scutellarin and ramification thereof in preparing medicine for preventing or treating diseases relevant with hepatofibrosis or preventing or treating hepatofibrosis caused by various reasons and preventing or treating hepatofibrosis caused by chronic liver disease, belonging to the technical filed of medicine. The invention shows that the scutellarin and scutelloside have hepatofibrosis-resisting function by cytology experiment and animal experiment; and the scutellarin and the scutelloside can be prepared into various pharmaceutical preparations for preventing and treating the chronic liver disease and the hepatofibrosis. The invention also relates to a method for preparing micropill of the scutellarin and the ramification thereof. The micropill substantially comprises 50-300 of scutellarin and ramification thereof, 50-1800 of polymer material and 0-300 of insoluble material. The polymer material selects from acrylicresins or/and ethyl cellulose and the ramification thereof. The viscosity range of the ethyl cellulose is 3-110 mPa.s, preferably is 20-50 mPa.s, and the insoluble material preferably selects from the micropill of silica gel.
US20100254998 Method for prolonging longevity The present application relates to a method for increasing the longevity of a subject by modulating a non-insulin-like neuropeptide receptor pathway. Preferably, said non-insulin-like neuropeptide receptor is the neuromedin U receptor 1 (NMUR1).
US20120129884 Photochemotherapeutic heterocyclic agents having antiproliferative and antineoplastic activity The present invention concerns the synthesis of new analogs of angelicins, pyrrolo [3,2-h]quinoline, for the treatment of pathologies having hyperproliferative character included those having neoplastic nature. The treatment is based on the combined action of pyrrolo [3,2-h]quinolines and UV-A light, through a clinical approach defined as PUVA (psoralen-UVA light). The most important feature of these compounds is that they exert their remarkable photoxicity without any DNA damage, which is the main origin of the side effects of the PUVA therapy.
WO2012029015A3 Anticaries dentifrice composition that includes anticaries propolis as an active principle The invention relates to a novel dentifrice composition having anticaries properties, including a combination of propolis, methylparaben, and propylparaben as an active principle. Of these three components, propolis is the main component, the effect thereof being strengthened by smaller amounts of methylparaben and propylparaben, resulting in a composition having high anticaries activity without harmful side effects. Said active components are present in the following percentages relative to the total weight of the dentifrice composition: 2 to 10% of propolis; 0.01 to 0.30% of methylparaben; and 0.01 to 0.15% of propylparaben, wherein the dentifrice composition further includes a fluoride compound and supplementary ingredients typical of such a formulation, such as abrasives, humectants, foaming agents, thickeners, sweeteners, flavorings, and deionized water.
CN102028825A Dental ulcer tablet containing dandelion and preparation method thereof The invention relates to a dental ulcer tablet containing dandelion, comprising a medicated adhering layer and a water-insoluble protective layer, wherein the medicated adhering layer comprises 0.1-15mg of extracts containing the dandelion, carbopol, borneol, low substituted hydroxypropy cellulose and sodium carboxymethylcellulose; the water-insoluble protective layer consists of ethyl cellulose and edible pigment; the extracts containing the dandelion consist of 8-10 grams of mint, 15-20 grams of dandelion, 5-10 grams of rush, and 10-15 grams of evodia rutaecarpa. The tablet medicament provided by the invention can fully improve local ulcer tissues and heal soon in order to attain the purpose of therapy. The Chinese patent medicine is innoxious and harmless to human bodies, and is convenient to take without decoction. The tablet seeks both temporary solution and permanent cure, and has significant clinical effects with effective rate of 98%.
US20090209633 Treatment of Pain With Resiniferatoxin and Related Analogs A method of treating inflammatory pain conditions is provided that involves administering an effective amount of a TRPV1 agonist, such as resiniferatoxin, tinyatoxin and related potent agonists and their analogs, to a patient to selectively induce nerve terminal depolarization block and/or nerve terminal death in select TRPV1-containing neurons, to provide the desired pain relief without significant permanent damage to cell bodies of the select TRPV-1 containing neurons.
EP2686312A1 N- cyclopropyl - n- piperidinylbenzamides as gpr119 modulators The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, Ar, m and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
EP1552836A1 Anti-neurodegenerative agents The present invention provides pharmaceutical agents useful for treatment and prevention of neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), spinal muscular atrophy (SMA), Huntington's disease, Parkinson's disease, Alzheimer's disease, dementia after cerebral vascular disorder, dementia accompanied by other neuronal degeneration. The agents comprise one, two or more compounds selected from the group consisting of 3-[4-(4-chlorophenyl) piperazin-1-yl]methyl]-1H-pyrrolo [2,3-b] pyridine or salts thereof, 5-(4-chlorophenyl)-4-methyl-3-(1-(2-phenylethyl) piperidin-4-yl) isoxazole or salts thereof, 3-(4-chlorophenyl)-4-methyl-5-(1-(2-phenylethyl) piperidin-4-yl) isoxazole or salts thereof, and N-methyl-4-(2-cyanophenyl) piperazinyl-3-methylbenzamine or salts thereof.
WO2008079387A1 Catechol protected levodopa diester prodrugs, compositions, and methods of use Catechol protected levodopa diester prodrugs pharmaceutical, compositions comprising catechol protected levodopa diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.
CN1853650A Calcium-supplementing agent A calcium supplementing capsules is composed of the water-soluble acidic shell and the calcium carbonate particles as filler, which can react on gastric hydrochloric acid to generate the easily absorptive calcium chloride and CO2 as natural disintegrant.
CN103083650A Composition with bone mineral density addition function, and preparation method as well as application of composition The invention relates to a composition with a bone mineral density addition function. The composition is prepared from the following raw materials in parts by weight of: 10-30 parts of D-glucosamine hydrochloride, 8-15 parts of chondroitin sulfate, 2-8 parts of collagen, 1-7 parts of a rhizoma drynariae extract, 1-7 parts of a horny goat weed extract, and 10-30 parts of milk calcium, and 10<-7> to 10<-5> parts of vitamin D3, wherein the mass content of calcium in the milk calcium is greater than or equal to 25%; the mass content of mucopolysaccharide in the collagen is greater than or equal to 25%; the horny goat weed extract contains not less than 10% by mass of icariin; and the rhizoma drynariae extract is an extract obtained from rhizoma drynariae dry rootstock through alcohol extraction. The composition has a reasonable formula design; the experiments prove that the composition has the bone mineral density addition function which is better than calcium carbonate. In addition, the composition with the bone mineral density addition function is simple in formula and low in cost, and the materials are easily available.
US7786147 used for the treatment of Parkinson's disease, Huntington disease, Alzheimer's disease, amyotrophic lateral sclerosis, spinal muscular atrophy, ataxia, Pick's disease, Pick's disease, vision defects, Cruetzfelt-Jacob syndrome or Alzheimer's disease The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected. Compounds according to the present invention are effective to alleviate and/or reverse the effects of a neurodegenerative condition, prevent further deterioration and/or enhance cognition and memory in patients suffering from neurodegenerative disorders, especially Alzheimer's disease.
US7893085 3-(4-Bromo-2-fluoro-phenylamino)-thieno[3,2-c]pyridine-2-carboxylic acid (2,2-dimethyl-[1,3]dioxolan-4-ylmethoxy)-amide; mitogen activated protein extracellular kinase kinase (MEK) inhibitor; antiproliferative, antiinflammatory agent The invention relates to azabenzothiophenyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzothiophenyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
CN103040816A Drug composition for curing peptic ulcer The invention discloses a drug composition for curing peptic ulcer and a preparation method thereof. The composition includes aldioxa, vitamin E acetate and silica, can be prepared into solid drug for oral medication through dry granulation, can be taken in the form of orally-taken solid drug, and can quickly release aldioxa for neutralizing gastric acid, protecting mucosa and resisting ulcer, at the same time, the vitamin E acetate in the composition is released in the mucosa to repair damaged mucosa, and the two drugs can be combined and taken for cooperative and synergistic action.
EP2059234B1 Method for reducing or alleviating inflammation in the digestive tract A method is provided for reducing or alleviating inflammation or a pathological process associated therewith or secondary thereto in a subject having an inflammatory disease of the digestive tract. The method comprises administering to the subject an anti-inflammatorily effective amount of an ACE2 inhibitor.
EP2067487A2 Immunomodulatory formulations and methods for use thereof The invention provides new compositions and methods for immunomodulation of individuals. Immunomodulation is accomplished by administration of immunomodulatory polynucleotide/microcarrier (IMP/MC) complexes. The IMP/MC complexes may be covalently or non-covalently bound, and feature a polynucleotide comprising at least one immunostimulatory sequence bound to a nonbiodegradable microcarrier or nanocarrier.
CN103054896A Compound dry suspension preparation containing omeprazole and sodium bicarbonate A compound dry suspension preparation containing omeprazole and sodium bicarbonate is characterized in that the sodium bicarbonate is adopted as buffer agent, and xanthan gum is adopted as suspending agent. The invention further relates to a preparation technique which relates to the particle size of xanthan gum.
US8088813 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine) An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid.
CA2540838A1 Process for the synchronization of ovulation for timed breeding without heat detection A method for synchronizing ovulation in sows and gilts by a single injection of hormones is disclosed. A hormone, gonadotropin releasing hormone (GnRH), luteinizing hormone (LH), follicle stimulating hormone (FSH), human chorionic gonadotropin (hCG), analogues, derivatives, agonists or combinations thereof is administered to an open sow post weaning at a specific time to stimulate ovulation of mature responsive follicles. The sow is then bred, without heat detection, at a specific subsequent timed interval after injection with hormone, with one or two artificial or natural breedings. In gilts, the hormone is injected at a timed interval from onset of estrus or at a specific timed interval following Prostaglandin F2a for those gilts which have been held in a state of pseudopregnancy.
US6916810 αν integrin receptor antagonists The present invention relates to cyclic urea derivatives, their synthesis, and their use as αv integrinreceptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αvβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, tumor growth and metastasis.
US20120156176 Thermoresponsive, biodegradable, elastomeric material and uses therefor Provided are novel biocompatible copolymers and compositions comprising the copolymers. The copolymers are non-toxic and typically have an LCST below 37° C. Compositions comprising the copolymers can be used for wound treatment, as a cellular growth matrix or niche and for injection into cardiac tissue to repair and mechanically support damaged tissue. The copolymers comprise numerous ester linkages so that the copolymers are erodeable in situ. Degradation products of the copolymers are soluble and non-toxic. The copolymers can be amine-reactive so that they can conjugate with proteins, such as collagen. Active ingredients, such as drugs, can be incorporated into compositions comprising the copolymers.
CN103585119A Stabilization preparation containing epoprostenol and medical salt of epoprostenol and preparation method of stabilization preparation The invention discloses a stabilization preparation containing epoprostenol and medical salt of epoprostenol and a preparation method of the stabilization preparation. Through preparation of an epoprostenol-cyclodextrin inclusion compound, the problems about the stability and the vascular stimulation of a conventional epoprostenol preparation are solved, the compliance of a patient is improved greatly, and the dosing stimulation is reduced. At the same time, the invention discloses the preparation method of the stabilization preparation containing epoprostenol and medical salt of epoprostenol; according to the preparation method, the preparation process is simple, the stability is high, the stimulation is low, and the safety is good; and the production cost is reduced, the stabilization preparation can be industrially prepared, and requirements for epoprostenol and medical salt of epoprostenol in clinical application are met.
CA2407683C Topical anesthetic/opioid formulations and uses thereof Many chemical and pharmaceutical compositions are known to produce antinociceptive effects that are helpful in relieving pain and inflammation. Both opioids and local anesthetics serve an important function in providing peripheral pain relief. Topical administration of pain-relieving drugs to the periphery offers important advantages over systemic or local, non-topical administration. The present invention provides topical pharmaceutical compositions, formulated with at least one local anesthetic and at least one opioid analgesic in a topical excipient. The present invention also provides methods for relieving pain in a subject through topical administration of the pharmaceutical composition in an amount and a duration sufficient to synergistically potentiate an antinociceptive response. Synergistic potentiation of analgesia through topical administration of a local anesthetic/opioid pharmaceutical composition provides a new and improved approach to peripheral pain management.
US20100041756 method of modulating b cell functioning The present invention relates generally to a method of modulating cellular functioning. More particularly, the present invention relates to a method of modulating B cell functioning, for example B cell proliferation, utilising an IDO-mediated tryptophan metabolite as herein defined (particular examples of such IDO-mediated tryptophan metabolites include 3-hydroxykynurenic acid, 3-hydroxyanthranilic acid, picolinic acid, quinolinic acid and tranilast). The method of the present invention is useful, inter alia, in the treatment and/or prophylaxis of conditions characterised by aberrant, unwanted or otherwise inappropriate B cell functioning such as antibody production, autoimmune conditions and B cell proliferation and neoplasias. In a related aspect, the present invention is directed to a method of therapeutically and/or prophylactically treating rheumatoid arthritis via the administration of the above-mentioned compounds.
CN103055321A Methoxy polyethylene glycol-polyphosphate diblock copolymer and adriamycin bonding medicine thereof The invention discloses a macromolecular bonding medicine based on adriamycin. The active ingredient of the bonding medicine is nanoparticles formed by bonding of a polyphosphate polymer and adriamycin. Specifically, the polyphosphate polymer can be a methoxy polyethylene glycol-polyphosphate diblock copolymer with amino as the side group. The invention also provides a methoxy polyethylene glycol-polyphosphate copolymer with an amino side group and a method for synthesizing the copolymer. The polyphosphate adriamycin macromolecular bonding medicine provided in the invention can self-assemble to form nanoparticles with a particle size of about 30nm. Through the intrinsic scale effect of the nanoparticles and by combining a charge reversal technology, the nanoparticles can better concentrate in a tumor tissues and a cell, thus enhancing the targeting property of adriamycin on a tumor site. And the adriamycin bonded on a polyphosphate polymer chain can have responsiveness to a tumor tissue microenvironment, and can be rapidly released in the tumor tissue under a weakly acidic condition. And a good tumor cell-killing effect can be achieved.
EP2101791A2 Anticonnexin polynucleotides as impaired wound healing compositions Connexin modulation for the treatment of wounds that do not heal at expected rates, including delayed healing wounds, incompletely healing wounds, and chronic wounds, and associated methods, compositions and articles.
EP0930894B1 Induction of rev and tat specific cytotoxic t-cells for prevention and treatment of human immunodeficiency virus (hiv) infection The presence of cytotoxic T-cells to the Rev and/or Tat protein in samples from a subject infected with immunodeficiency virus, particularly HIV in humans, is an indication of a stable disease condition and a favourable prognosis of lack of progression to disease. Immunogenic compositions containing at least one cytotoxic T-cell epitope of the Rev and/or Tat protein of an immunodeficiency virus, particularly HIV, or a vector encoding the T-cell epitope, may be used to prevent infection by disease caused by the immunodeficiency virus, by stimulating, in the host, a specific cytotoxic T-cell response specific for the respective Rev and/or Tat proteins.
CN102329360A Dammar-20S, 25R-epoxy-3beta, 12beta, 26-triol and extraction method and drug use thereof The invention relates to a dammar-20S, 25R-epoxy-3beta, 12beta, 26-triol and an extraction method and drug application thereof, belonging to the field of novel compounds and drug application thereof. Red ginsengs are used as raw materials and a novel compound is obtained through alcohol extraction, normal and reverse phase silica gel column chromatography and re-crystallization, wherein the chemical name of the novel compound is dammar-20S, 25R-epoxy-3beta, 12beta, 26-triol. The yield reaches more than 0.03 percent. The dammar-20S, 25R-epoxy-3beta, 12beta, 26-triol can be widely used for preparing anti-tumor drugs.
WO2014027209A1 Pyrazolyl-ureas as kinase inhibitors There are provided compounds of formula I, wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
WO2012006938A1 Pharmaceutical composition capable of targeted release of trace element, and preparation method and application of pharmaceutical composition A pharmaceutical composition having an effect of ultrasound targeted release of a trace element comprises hollow microspheres having a particle size of less than 10 μm at a concentration of higher than 1x106/ml, at least one trace element at a concentration of less than or equal to ten times the physiological dose of a human body, and a pharmaceutically acceptable carrier or excipient. The trace element and the hollow microspheres exist in a manner of combination, and the hollow microspheres are prepared by a pharmaceutically acceptable film forming material.
EP2501378A1 Use of macrocyclic lactone derivatives for the treatment of inflammatory disorders The present invention provides use of the compounds represented by formula (1): wherein, R1, R2, R3 and R4 are as defined in the specification, in all their stereo isomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs and pharmaceutical compositions containing them for treatment of inflammatory disorders mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-α), interferon-γ (IFN-γ) and interleukins such as IL-lβ, IL-2, IL-6, and IL-8. The present invention also relates to a pharmaceutical composition adapted for use in the treatment of inflammatory disorders. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.
WO2011114275A1 Spirocyclic compounds and their use as therapeutic agents and diagnostic probes The invention relates to new triazines (G = Q = U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E1 is CR4 or N; X1 is CHR4, CH2CH2, NR4, NR4→0, or O; and the other substituents are as defined in the specification. The compounds inhibit phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR), DNA-PK and ATM kinase, and may be used as therapeutic agents or diagnostic probes. The invention also relates to methods of using the compounds for treatment of associated pathological conditions.
EP2076289A2 Methods for treating cancer resistant to erbb therapeutics Provided herein are methods for treating cancer that is resistant to treatment with an anti- ErbB therapeutic agent and which is associated with an activating MET gene mutation or a MET gene amplification. The methods involve administering to a subject a combination of an anti- ErbB therapeutic and an anti-MET therapeutic. Also provided are methods for reducing ErbB mediated signaling or PI3 kinase mediated signaling in a cancer cell.
US7371772 Bicyclic compound, production and use thereof The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
EP1307588B1 Method for diagnosing or determining a risk for psychosis comprising determining an heterozygous mutation of methylenetetrahydrofolate reductase (MTHFR) The invention features methods for diagnosing subjects at risk for or suffering from a disease or disorder, such as a psychosis. Methods are also provided for selecting a preferred therapy for a particular subject or group of subjects.
CN101623262B Cephazolin sodium pentahydrate proliposome preparation The invention provides a cephazolin sodium pentahydrate proliposome preparation which comprises the following components by weight part: 5-15 parts of cephazolin sodium pentahydrate, 10-50 parts of lecithin phosphatidylserine, 1-20 parts of cholesterol and 5-40 parts of proppant which consists of two or more of mannitol, lactose, glucose, trehalose, sucrose, dextran, sorbitol, sodium chloride, glycine and hydrolyzed gelatin. The cephazolin sodium pentahydrate proliposome has good stability and cannot crack because of dewatering, fusion, ice crystal generation, and the like in a drying process; and after hydrated re-dissolution, the entrapment rate of the cephazolin sodium pentahydrate proliposome cannot be reduced.
CN103637990A Method for preparing folic acid coupled chitosan-hydrochloric acid mitoxantrone nano-particle The invention relates to the technical field of tumor targeted medicaments, and in particular relates to a method for preparing a folic acid coupled chitosan-hydrochloric acid mitoxantrone nano-particle. The method comprises the following steps: 1, mixing a hydrochloric acid mitoxantrone solution with chitosan acetum so as to obtain a mixture solution of chitosan and hydrochloric acid mitoxantrone; 2, adding the mixture solution of chitosan and hydrochloric acid mitoxantrone into a folic acid amino solution, subsequently continuing adding a polysodium phosphate solution into the folic acid amino solution, and uniformly mixing so as to obtain a folic acid-chitosan-hydrochloric acid mitoxantrone microsphere water dispersed system; 3, centrifuging the acid-chitosan-hydrochloric acid mitoxantrone microsphere water dispersed system so as to obtain precipitate, washing the precipitate, and subsequently freezing to dry and obtain the folic acid coupled chitosan-hydrochloric acid mitoxantrone nano-particle. By adopting the method, application of an organic solvent is prevented, the reaction time is greatly shortened, and the prepared nano-particle has a remarkable targeting function on tumor cells, and is good in biocompatibility.
WO2010020057A1 Treatment and/or Prevention of Peanut Induced Anaphylaxis Compositions and methods for the treatment of food allergies, particularly peanut allergy are provided. The compositions and methods are based on the observation that agents which interfere with the association of platelet activating fact (PAF) with its receptor (PAF-R) significantly reduce the severity and duration of anaphylaxis. Combination therapy with a PAF inhibitor and a histamine inhibitor provided an increased beneficial effect compared to treatment alone.
US7652144 Compounds as PDE IV and TNF inhibitors A compound of formula XIX wherein R1, R2, Z1, Z2, Q1, Q2 and Q3 as defined in the specification.
CN103108863A Production of atorvastatin low in ether impurities The present invention relates to a method for the production of atorvastatin having decreased levels of impurities of general formulae (3) and (4) by means of a concentrating step.
WO2013105057A1 Fused pyrroles as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Formula (1a) (1b)
WO2008008608A3 Method of treating and preventing secondary hyperparathyroidism A method of treating elevated blood levels of iPTH by increasing or maintaining blood concentrations of both 25 -hydroxy vitamin D and 1, 25-dihydroxyvitamin D in a patient by administering, as necessary, both Vitamin D repletion and Vitamin D hormone replacement therapies, is disclosed. The blood concentrations of 25 -hydroxy vitamin D are increased to and maintained at or above 30 ng/mL, and blood concentrations of 1, 25-dihydroxyvitamin D are increased to or maintained within a patient's normal historical physiological range for 1, 25-dihydroxyvitamin D without causing substantially increased risk of hypercalcemia, hyperphosphatemia or over suppression of plasma iPTH in the patient. The blood levels of 25- hydroxyvitamin D are maintained at or above 30 ng/mL between doses of Vitamin D repletion therapies, and the blood levels of 1, 25-dihydroxyvitamin D are maintained in the patient's normal historical physiological range between doses of Vitamin D hormone replacement therapies. In one aspect, the disclosure includes methods wherein the blood concentration of 25- hydroxyvitamin D during treatment comprises predominantly 25 -hydroxy vitamin D3, and/or wherein the method includes administering predominantly or solely 25-hydroxyvitamin D3 for 25 -hydroxy vitamin D repletion and/or maintenance
CN102247401A Low molecular weight glycosylated chondroitin sulfate and its purpose in preparation of anti-HIV-1 medicament The invention discloses a low molecular weight glycosylated chondroitin sulfate, whose weight average molecular weight is 3000-15000Da. The monosaccharide composition comprises acetyl galactosamine (D-GalNAc), glucuronic acid (D-GlcUA), fucose (L-Fuc), or its sulfuric ester (expressed in -OS03<->), wherein the mole ratio of D-GalNAc to D-GlcUA to L-Fuc to -OS03<-> is 1: (1+/-0.3): (1+/-0.3): (3.5+/-0.5). The low molecular weight glycosylated chondroitin sulfate has a strong anti-HIV-1 virus activity, is a gp120 entry inhibitor, and can be used for preventing and/or treating AIDS. The invention also provides a method for preparing the low molecular weight glycosylated chondroitin sulfate and its composition preparation. Glycosylated chondroitin sulfate is depolymerized by the peroxide method to obtain a low molecular weight product, and then low molecular and/or high-molecular impurities of the product are removed by gel separation or ultrafiltration method. The low molecular weight glycosylated chondroitin sulfate and its medicinal composition can be prepared in the form of an injection, a lyophilized powder or a suppository.
US20120220537 9-aminoacridine derivatives, their preparation and uses N-substituted 9-aminoacridine and bis-acridino derivatives containing electron-withdrawing groups (EWG) or electron-donating groups (EDG), including amino acid residues, and one-pot methods for their synthesis are disclosed. The derivatives are potential candidates for cancer treatment.
US20110178054 Heterocyclic GPCR Agonists Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR (GPR119) agonists and are useful as for the treatment of diabetes and obesity.
US20110190288 Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) for use in treatment of diseases associated with a pten deficiency A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions associated with a PTEN deficiency that are ameliorated by the inhibition of PARP activity.
WO2009050183A2 Imidazo [1, 2-a] pyridine derivatives useful as alk inhibitors Compounds of formula I: in free or salt or solvate form, where R1, R2, R3 and R20 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described. These compounds are useful for the treatment of inflammatory or obstructive airways diseases such as pulmonary hypertension, pulmonary fibrosis, liver fibrosis, cancer, muscle diseases such as muscle atrophies and muscle dystrophies, and systemic skeletal disorders such as osteoporosis.
US20120015962 PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
CN101301383A Quality control method of formulation for clearing wind-heat of children The invention discloses a method for controlling the quality of children Fengreqing mixture. The method adopts the high performance liquid chromatography to measure the content of geniposide contained in the children Fengreqing mixture and identify a plurality of effective components; the method achieves higher standards according to national standards of the National Institute For the Control of Pharmaceutical and Biological Products, so that the method has the advantages of being easily operated, saving measuring costs and lowering the toxicity of the reagent.
CN101856353A Medicinal composition using tolperisone optical isomer as active ingredient The invention relates to a medicinal composition using a tolperisone optical isomer as a main ingredient, which is a medicinal preparation prepared from the tolperisone optical isomer and pharmaceutically acceptable auxiliary materials through a preparation technique. Compared with a racemate, the tolperisone using a single optical isomer has a better curative effect and a lower toxic and side effect. The oral tolperisone optical isomer medicinal composition has the advantages of stable quality, controllability, safety and effectiveness.
CN102603685A Flavonoid fatty acid ester derivatives, preparation method and medicinal use of flavonoid fatty acid ester derivatives The invention relates to the field of pharmaceutical chemistry, in particular to flavonoid fatty acid ester derivatives as shown in a formula (I), or (II) or (III), a preparation method of the flavonoid fatty acid ester derivatives and a medicinal use of the flavonoid fatty acid ester derivatives, particularly the use of the flavonoid fatty acid ester derivatives as drugs for preventing or treating obesity, hyperlipaemia and II-type diabetes.
WO2014161412A1 Tricyclic quinolone derivative and preparation method and use thereof Disclose in the invention are a tricyclic quinolone derivative having a novel structure with a peripheral group at position C10 being substituted by non-alkaline substituents or salts and hydrates thereof. Such compounds have been proven to have anti-microbial activity against a variety of sensitive strains and drug-resistant strains through activity assays made on various strains, and can be used for treating infectious diseases caused by gram-negative and gram-positive bacteria, in particular being suitable for treating diseases caused by methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa infections.
US6927219 Secondary amides such as N-Adamantan-1-methyl-2-chloro-5-(3,5-dioxo-4,5-dihydro-3H- (1,2,4)triazin-2-yl)-benzamide used as antagonists for biological receptors; antiinflammatiory, anticarcinogenic or antiischemic agents The present invention relates to novel to N-alkyl adamantyl triazinyl benzylamide derivatives of formmula I: and to processs for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them, and their use in therapy. The active compounds of the present invention are useful in the treatment of inflammation, osteoarthritis, rhematoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
US20060067938 Methods for the treatment of osteoarthritis and compositions thereof The invention discloses PI3K, PKB, IL-1, and OSM as suitable targets for the development of new therapeutics to treat, prevent or ameliorate osteoarthritis (OA). The invention relates to methods to treat, prevent or ameliorate OA and pharmaceutical compositions therefor comprising substances with inhibitory effects on PI3K and/or PKB enzyme activity and/or gene expression and IL-1 and/or OSM activity or gene expression. The invention also relates to a method to identify compounds with therapeutic usefulness to treat OA, comprising identifying compounds that can effect PI3K and/or PKB activity and/or gene expression and/or IL-1 or OSM activation of PI3K and/or PKB activity and/or gene expression which leads to downregulation of AGG-1 and/or COL-3 and thus prevent, treat or ameliorate OA in vivo.
EP1224188B1 Nasal delivery composition comprising the methane sulphonate salt of morphine and chitosan The methane sulphonate salt of morphine and compositions thereof are described. Also described is a composition adapted for nasal delivery comprising a methane sulphonate salt of an opioid analgesic.
US20080039519 Anti-Demodicosis Agent The present invention relates to the use of macrocyclic lactones for treating demodicosis, particularly in dogs.
CN1997619B Phenyl derivatives comprising an acetylene group This invention is concerned with compounds of the formula (I) wherein one of R5, R6 and R7 is formula (II) and X1, X2, R1 to R12, m, n and o are as defined in the description, and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPARd and/or PPARa agonists.
US7351429 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide as an active ingredient, excipient, binder, lubricant and coating agent; uniform in the content of a small amount of active ingredient, excellent light stability; anticholinergic activity on bladder and drug for pollakiuria and urinary incontinence The invention is to provide an oral solid pharmaceutical that is uniform in the content of KRP-197, having bladder-selective anticholinergic activity, being a therapeutic drug for pollakiuria and urinary incontinence, and being active with a very low dosage, that can be taken quantitatively, and that is easy in the handling. Since KRP-197 becomes unstable to light under the influence of additives, the invention is to select the additives to be used and to obtain a pharmaceutical with high stability. By formulating KRP-197 with drug-making carriers, a pharmaceutical that is uniform in the content, capable of taking quantitatively and easy in the handling has been provided. Furthermore, by using polyvinyl pyrrolidone for binder and by making into tablet coated with a coating base containing titanium dioxide and ferric oxide, a pharmaceutical capable of taking quantitatively and excellent in the light stability has been provided.
US20080318914 Treating a traumatic brain injury by administering progesterone; dosing regime is constant or two-level, e.g., administering a higher hourly dose followed by a second time period during which a lower hourly dose is administered Methods of treating a subject with a traumatic central nervous system injury, more particularly, a traumatic brain injury, are provided. The methods comprise a therapy comprising a constant or a two-level dosing regime of progesterone. In one method, a subject in need thereof is administered at least one cycle of therapy, wherein the cycle of therapy comprises administering a therapeutically effective two-level intravenous dosing regime of progesterone. The two-level dosing regime comprises a first time period, wherein a higher hourly dose of progesterone is administered to the subject, followed by a second time period, wherein a lower hourly dose of progesterone is administered to the subject.
WO2013189862A1 Substituted pyrazole compounds as lpar antagonists Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis
CN102204883B Promethazine hydrochloride microenema prescription and preparation method thereof The invention discloses a promethazine hydrochloride microenema prescription and a preparation method thereof. The preparation method comprises the following steps of: dissolving hydroxypropyl methylcellulose, or polyethylene glycol 6000 or polyvinylpyrrolidone in purified water to form a solution A; dissolving sodium bisulfite, sodium sulfite, vitamin C and EDTA-2Na (Ethylene Diamine TetraaceticAcid-2Na) in purified water, then adding promethazine hydrochloride and dissolving to form a solution B; dissolving ethylparaben in a small amount of boiled water to form a solution C; and adding thesolution C to the solution B to form a solution D, adding the solution D to the solution A, stirring and adding purified water to form a solution and stirring evenly, inspecting and subpackaging. Thepromethazine hydrochloride microenema prescription is convenient to use, is easy to adjust the administration dose to adapt to sick children of different ages, and has better clinical applicability and convenience, thereby ensuring safe and reasonable medication; and the promethazine hydrochloride microenema prescription can overcome the defect in convenience of tablets and rectal suppositories in dose adjustment and the like, overcomes the defect of syrup in stability, is especially applicable to pediatric patients, and is easy to adjust the dose according to the condition of patients to meet the individual requirement on treatment.
US20130018081 AChE ANTISENSE OLIGONUCLEOTIDE AS AN ANTI-INFLAMMATORY AGENT Disclosed is a novel use for AChE antisense oligonucleotides as anti-inflammatory agents, wherein said oligonucleotides are preferably as denoted by SEQ ID NO:1, SEQ ID NO:2 and SEQ ID NO:7. Methods of treatment of inflammatory conditions, as well as fever, and particularly inflammation-associated neuropathies such as Guillain-Barré Syndrome, are described.
US6869959 Heterocyclic carboxylic acid derivatives Compounds or salts thereof represented by the formula (I) wherein R1 represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkenyl group, or an acyl group, R2 and R3 represent hydrogen atom or a C1-6 alkyl group, or adjacent R2 and R3 may combine to form 5- to 7-membered ring, R4 represents hydrogen atom, hydroxyl group, a C1-6 alkoxyl group, a C1-6 alkyl group, HAr represents a heteroaryl-diyl group consisting of a 5-membered or 6-membered ring containing 1 to 3 hetero atoms, R5 represents hydrogen atom or a C1-6 alkyl group. The compounds or the salts thereof have retinoid-like physiological activities or controlling activity on physiological activities of retinoid.
WO2007053082A1 Novel 1 -benzyl-4-piperidinamines that are useful in the treatment of copd and asthma The invention provides 1 -benzyl- 4 -piperidinamines of the general formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory diseses such as chronic obstructive pulmonary disease and asthma. The compounds are inhibitors of the CCRl receptor.
US20080070888 Spirocyclic azetidin(one); 2-(3-chloro-4-fluorophenyl)-7-[5-fluoro-6-(trifluoromethyl)-1H-benzimidazol-2-yl]-3-(2-pyridinyl)-2,7-diazaspiro[3.5]nonan-1-one; T-type calcium channel blockers Disclosed are compounds of the formula wherein Z1 is —CH2— or —C(O)—, R4 and R5 are carbon chains (and optionally, together can form a C2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R1 and R3 are as defined herein. Also disclosed are methods of treating pain using a compound of formula I.
WO2014011768A1 Anti-anxiety treatment The present invention relates to methods of using select small molecule and aptamer ligands that bind to a regulatory (binding site on nicotinic acetylcholine receptors to treat or to prevent anxiety behavior and symptoms, such as but not limited to, the following categories of disorders: dissociative, eating, impulse - control, adjustment, anxiety, mood, personality, psychotic, post-traumatic stress, sexual, sleep-related, and somatoform, in a subject.
US20120108507 Methods for In Vivo Cell Reprogramming The present disclosure provides a new technology platform that converts one type of cells (substrate cells) to another type of cells (product cells).
CN1989973A Application of amygdalin in preparation of amygdalin preparation for promoting the blood circulation of heart, brain, pancreas and wound The invention discloses the use of bitter apricot seed glycosides in preparing preparations for blood circulation of heart, brain, pancreas and wound positions, wherein the preparation can be used for preventing and treating cerebral ischemia, cardiac function prostration, acute adenitis, for promoting skin tissue microcirculation blood flow and wound healing.
US8609695 Methods of treating and/or suppressing insulin resistance Novel methods for the medical treatment and/or prevention of obesity, abdominal fat, and insulin resistance in susceptible warm-blooded animals including humans involves the administration of selective estrogen receptor modulators (SERMs). A combination of a SERM with an amount of estrogen or a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3b,17b-diol and compounds converted in vivo to one of the foregoing precursors or estrogen is also disclosed.
EP1539227A2 Papaine containing pharmaceutical formulation resp. its use The present invention refers to a pharmaceutical composition applied to treat the Peyronie disease and the collagenous and fibrotic pathologies and its corresponding obtainment process. The composition comprises in its formulation papaine and eventually vitamin-E and/or hyaluronidase.
CN101984975A Medical composition containing cordycepin derivatives The invention relates to a medical composition, which is prepared by combining medical salts of cordycepin serving as active components with pharmaceutically acceptable auxiliary materials. The composition can be prepared into clinically oral liquid preparations and injection preparations, and can be used for preparing drugs such as antitumor drugs, anti-infective drugs, immune regulation drugs, antilipemic drugs, antifatigue drugs and the like.
CN102949375A Berberine hydrochloride solid lipid nano preparation and preparation method thereof The invention discloses a berberine hydrochloride solid lipid nano preparation and a preparation method thereof, relates to berberine hydrochloride, and provides the berberine hydrochloride solid lipid nano preparation which has the advantages of simple method, low production cost, convenience in carrying and transportation and suitability for any administration route and the preparation method thereof. The berberine hydrochloride solid lipid nano preparation comprises the following raw materials in percentage by mass: 1 percent of berberine hydrochloride, 5-15 percent of solid lipid, 5-15 percent of emulsifier and 1-3 percent of surfactant. The solid lipid and the emulsifier are added into an organic solvent; after the solid lipid is fully dissolved, the berberine hydrochloride is added and is dissolved to obtain an oil phase; the obtained oil phase is added into a water phase containing the surfactant and is stirred until the organic solvent is fully removed; the obtained material is subjected to ultrasonography, is cooled and then is filtered by using a micro-porous filter membrane to obtain berberine hydrochloride solid lipid nanoparticle suspension; and the obtained berberine hydrochloride solid lipid nanoparticle suspension is added into a free-dry protecting agent to be freeze-dried to obtain the berberine hydrochloride solid lipid nano preparation which is in the form of nanoparticle freeze-dried powder.
US8758777 Pharmaceutical compositions comprising water-soluble sulfonate-protected nanoparticles and uses thereof The present invention provides pharmaceutical compositions comprising water-soluble sulfonate-protected nanoparticles, more particularly, pharmaceutical compositions comprising water-soluble sulfonate-protected silver or gold nanoparticles. The pharmaceutical compositions of the invention are useful in prevention or treatment of infections or conditions or disorders caused by microorganisms capable of binding to heparan sulfate, e.g., herpes simplex viruses.
US20120213766 Anticancer Compounds from Vernonia Guineensis This invention relates to novel compounds with anticancer activity isolated from Vernonia guineensis (Asteraceae) having chemotherapeutic activity against abnormal cell growth such as cancers. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating abnormal cell growth such as cancer, including combination therapies thereof.
CN1899472A Night oral administration Tibet medicine for treating diabetes and its preparing method The night taken Tibetan medicine for treating diabetes is prepared with bear bile, emblic, saffron, artificial musk, amur barberry bark and other four kinds of medicinal materials, and through grinding into fine powder and mixing in certain weight proportion. It may be prepared into bolus, medicine powder, soft capsule or granule. The Tibetan medicine can lower blood sugar and lower serum triglyceride, and has also obvious curative effect on nephrosis. It has fast absorption of the effective components in the medicine and high curative effect.
US20080166425 Suppressing cellular cyclin D1 overexpression; mantle cell lymphoma; activating glycogen synthase kinase 3 beta and I kappa B kinase phosphorylation and ubiquitination for proteasome degradation The invention provides a method for treating cancers that are dependent on cyclin D1 for proliferation, survival, metastasis and differentiation, involving administering a composition containing an effective amount of arsenic trioxide to an affected patient. The arsenic trioxide can be administered orally, for example, as a solution, suspension, syrup, emulsion, tablet, or capsule. The composition can also contain one or more pharmaceutically acceptable carriers and/or excipients.
WO2014037727A1 Carcainium salts A pharmaceutically acceptable addition salt of (i) carcainium, and (ii) oxalic acid, fumaric acid, maleic acid orhydrobromic acid.
CN101019880A Nanometer liver targeting floxuridine powder for injection and its prepn The present invention discloses one kind of nanometer liver targeting floxuridine for injection. The nanometer liver targeting floxuridine for injection consists of floxuridine diester 1-5 wt%, galactoside 0.5-1 wt%, soybean lecithin 10-20 wt% and mannitol for the rest. It is prepared through film ultrasonic and other process, and has medicine carrying amount of 8.2-10.0 %, encapsulating rate 90-98.5 % and granularity of 90-150 nm. Animal test shows that it has targeting efficiency of vein administration over 10. The present invention is used in treating primary liver cancer, and the effective medicine molecules are concentrated in liver. Compared with common preparation, the present invention has reduced medicine consumption and reduced toxic side effect.
US20100081718 Combinations comprising alpha-2-delta ligands The instant invention relates to a combination, particularly a synergistic combination, of an alpha-2-delta ligand and a dual serotonin-noradrenaline re-uptake inhibitor (DSNRI) or one or both of a selective serotonin re-uptake inhibitor (SSRI) and a selective noradrenaline re-uptake inhibitor (SNRI), and pharmaceutically acceptable salths thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.
US20080267901 Biocompatible Polymer Networks Functionalized prepolymers and biocompatible polymer networks are disclosed, especially biodegradable polymer networks obtainable by polymerization of the functionalized prepolymers by for example ultraviolet (UV), redox, and/or heat radical polymerization. Functionalized prepolymers (macromers) are obtainable by reaction of a prepolymer comprising at least one alcohol, amine, and/or sulfhydril group, with an unsaturated mono-esterified dicarbonic acid, especially fumaric acid mono-ethyl ester.
CN103494778A Esomeprazole sodium freeze-dried preparation and preparation method thereof The invention discloses an esomeprazole sodium freeze-dried preparation prepared by freeze-drying a liquid medicine which is prepared by dissolving esomeprazole sodium, alkaline amino acid and sodium hydroxide in water for injection, wherein the contents by mass volume ratio of the someprazole sodium, the alkaline amino acid and the sodium hydroxide are as follows: 20 mg/ml of the someprazole solidum, 0.5-5 mg/ml of the alkaline amino acid and the sodium hydroxide which adjusts the pH value of the liquid medicine within 11.0-12.0. As the alkaline amino acid is adopted as a stabilizing agent, amino bond existing in the alkaline amino acid can improve stability of the esomeprazole sodium in the processes of dissolution, freeze-drying, and storage. However, as alkaline amino acid is essential amino acid for a human body, the disclosed esomeprazole sodium freeze-dried preparation has higher safety in comparison with the existing esomeprazole sodium freeze-dried preparations which almost adopt edetic acid and salts of edetic acid as the stabilizing agent.
EP1696893A1 Continuous combination therapy with selective prostaglandin ep4, receptor agonists and an estrogen for the treatment of conditions that present with low bone mass. This invention is directed to methods for treating conditions which present with low bone mass in a patient in need thereof using continuous combination therapy with a synergistically effective combination of an EP4 receptor selective agonist or a pharmaceutically acceptable salt thereof, such as 5-(3-{2S-[3R-hydroxy4-(3-trifluoromethyl-phenyl)-butyl]-5-oxo-pyrrolid in-1-yl}-propyl)-thiophene-2carboxylic acid or a pharmaceutically acceptable salt thereof; and an estrogen or a pharmaceutically effective salt thereof. The present methods are useful for treating conditions that present with low bone mass including osteoporosis, osteotomy, osteoporotic fracture, childhood idiopathic bone loss, periodontitis and low bone mass and for enhancing bone healing following facial reconstruction, maxillary reconstruction or mandibular reconstruction, inducing vertebral synostosis, enhancing long bone extension, enhancing the healing rate of a bone graft or a long bone fracture or enhancing prosthetic ingrowth in a patient in need thereof.
CN102552447A Integrated novel dosage form preparation technology of Achyranthes bidentata decoction and production method thereof The invention relates to an integrated novel dosage form preparation technology of an Achyranthes bidentata decoction and a production method thereof. The effective components comprise 8 weight parts of talcum, 6 weight parts of Angelica sinensis, and 6 weight parts of Caulis Akebiae, 4 weight parts of Achyranthes bidentata, 4 weight parts of Dianthus superbus, and 5 weight parts of cluster mallow fruit. The production process comprises the steps of ultrasonic air-flow crushing, alcohol and aqua abstraction, supersonic crushing extraction, water decoction condensation, ultrasonic spray drying, nano grinding, high pressure homogenization, nano particle preparation, etc. According to the invention, the invention emphasizes to use the advantages of multi-synergy, multi-targeting, etc. of the nano carrier coupling techinique, thus after large scale production, the production cost can be greatly reduced, the product quality can be greatly raised, and the targeting and sustained and controlled release of the medicine are strong; the prepared dosage form of the decoction can combine internal and external administration, can be taken in four time periods according to the time of the midnight-noon and ebb-flow doctrine, and the human qi-blood flow rule, and can be made into films and transdermal agent that can be directly absorbed by skins to be respectively pasted on different positions of the human body according to the time of the midnight-noon and ebb-flow doctrine, and the human qi-blood flow rule.
CN101002778A Injection containing anti-infective, and its preparation method An injection of the quinolone medicine for treating infection is prepared from the medicine A and water or physiological saline or glucose solution. Said medicine A is 6-fluoro-1-methyl, 4-oxy-7-(1-piperazinyl)-4H-[1, 3] thiazine [3, 2-a] quinoline- 3-carboxylate.
CN102716089B Gemcitabine hydrochloride liposome injection The invention discloses a gemcitabine hydrochloride liposome injection and a preparation method thereof. The gemcitabine hydrochloride liposome injection is prepared from the following components in specific percentage by weight: gemcitabine hydrochloride, cholesterol, egg yolk phosphatidylinositol, phosphatidylcholine, tween 80, trehalose, mannitol and polyvinylpyrrolidone. The liposome injection is high in stability and cannot be cracked due to fusion, ice crystal and the like during freezing; and after long-term storage, liposome is still high in package rate. According to the gemcitabine hydrochloride liposome injection, the solubility of gemcitabine hydrochloride is improved; the quality of a product is improved; the toxic and side effects are reduced; the retention time of medicines during general circulation is prolonged; the biological utilization rate of the medicine is increased; the treating effect is obviously enhanced; the preparation method is simple; and the gemcitabine hydrochloride liposome injection is suitable for industrial large-scale production.
WO2006060082A1 Tricyclic compounds, preparation thereof and use thereof as cholinesterase activity inhibitors Described herein are tricyclic compounds of formula (I) and (II) and methods of making them and using them as cholinesterase activity inhibitors.
US20110300238 Mixture of inorganic compounds, preparations containing the mixture and use of the mixture A mineral mixture including at least' MgO and its equilibrium of Mg(OH)2, and MgCl2, in which MgO—Mg(OH)2 constitutes between 85 and 99.99% by weight; and MgCl2 constitutes between 0.01 and 15% by weight of the magnesium compounds in the mineral mixture. Preparations containing the salt mixture and the use of the mineral mixture for the production of a pharmaceutical preparation for the prevention or therapy of a condition, the condition being undesired eczema or psoriasis, are also described.
CN102091058A Medical application of 6-shogaol for treating cervical cancer The invention relates to the field of natural drugs, in particular to a medical application of 6-shogaol for treating cervical cancer. The research on the pharmacological activity of the 6-shogaol shows that: although the 6-shogaol has a curative activity on various kinds of tumors, the activity on different tumors has great difference. In multiple tumor-inhibiting tests, the 6-shogaol has a best effect on treating cervical cancer, breast cancer and leukemia, i.e. the effect on treating cervical cancer, breast cancer and leukemia by using the 6-shogaol is obviously better than the effect on treating other kinds of cancers by using the 6-shogaol.
EP1246627B1 Polyanhydrides with biologically active degradation products Polyanhydrides which degrade into biologically active salicylates and alpha-hydroxy acids and methods of using these polyanhydrides to deliver the salicylates and alphahydroxy acids to a host are provided.
US20110251205 Squaramide derivatives as cxcr2 antagonist The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
EP2105442A1 Method for producing c-glycoside derivative and synthetic intermediate thereof The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.
CN103622969A Application of chiral spiro indole-pyran pyrimidine base compound in preparation of anti-inflammatory drugs The invention provides a new medical application of a chiral spiro indole-pyran pyrimidine base compound, particularly application of the compound in preparation of anti-inflammatory drugs. An in vitro cyclooxygenase (COX) activity inhibiting experiment, an experiment of inhibiting generation of an inflammatory molecule (nitric oxide) in primary mice macrophage and inhibition test on an ear swelling and paw edema model in mice, show that the chiral compound has an obvious anti-inflammatory effect and has extremely low gastrointestinal injury effect; therefore, the chiral compound, as an active ingredient, can be prepared into anti-inflammatory drugs in various dosage forms through pharmaceutically acceptable technologies and auxiliary materials, so that the chiral compound has an excellent medical application prospect.
CN103518968A Feed additive for controlling avian iluenza The invention discloses a feed additive for controlling avian iluenza. The additive needed for preparing 100kg of feed is prepared from the following active ingredients by weight: 30-50g of dandelion, 20-40g of folium phyllostachys, 20-40g of achyranthes aspera, 20-40g of belamcanda sinensis, 10-30g of gypsum, 10-30g of selfheal, 10-30g of scutellaria baicalensis, 10-30g of fructus forsythiae, 10-30g of lobelia chinensis, 10-30g of dahurian patrinia herb, 10-30g of radix paeoniae rubra, 10-30g of platycladi seed, 10-30g of paniculate swallowwort root, 10-20g of fructus amomi, 5-10g of amantadine and 5-10g of sulfadiazine sodium. The feed additive is simple in proportioning, is convenient to use and has good control effects and few drug residues.
CN101972260B Rosuvastatin calcium oral drug composition The invention relates to a rosuvastatin calcium oral drug composition and a preparation method thereof. The rosuvastatin calcium oral drug composition is characterized by comprising the following components in proportion: 10-80mg of rosuvastatin calcium, 20-160mg of hydroxypropyl betadex, 5-40mg of meglumine, 2-16mg of sodium sulfite, 100-800mg of lactose, 50-400mg of microcrystalline cellulose, 20-160mg of croscarmellose sodium, 2-16mg of magnesium stearate and a proper amount of 80 percent ethanol solution. The preparation method comprises the following steps of: dissolving hydroxypropyl betadex, meglumine and magnesium stearate into a proper amount of 80% ethanol solution; adding rosuvastatin calcium and mixing until the rosuvastatin calcium is completely dissolved; evenly mixing lactose, microcrystalline cellulose and croscarmellose sodium for later use; quantitatively adding the solution into an evenly-mixed accessory for pelletization; and obtaining a finished product by drying, palletizing, totally mixing, checking an intermediate body, pressing into pieces, coating and packing. The prepared rosuvastatin calcium tablet has good stability and high bioavailability.
CN101322703A Granisetron hydrochloride mouth spray The invention provides a spray preparation made by mixing granisetron hydrochloride, a pharmaceutically acceptable adjuvant and water for buccal delivery.
EP2396313A1 Isotopologues of thalidomide Provided herein are thalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.
US6994957 Using nucleic acid The invention provides NAIP nucleic acid and sequences. Also provided are anti-NAIP antibodies and methods for modulating apoptosis and detecting compounds which modulate apoptosis.
WO2007042465A3 Combinati0n of nilotinib with farnesyl transferase inhibitors The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) an farnesyl transferase kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.
US20110021526 Pharmaceutical Composition for Treatment of Diabetic Complications A method for treating diabetic complications by administration of a beta-blocker is disclosed. Diabetic complications arise from diabetes and have few or no existing treatment options. The present invention describes the use of a beta-blocker in the treatment of a diabetic. The present invention also describes the inhibition of aldose reductase, one of the chief causative factors of diabetic complications. Also provided are methods of diabetic wound healing. Compositions for treating diabetic complications, such as diabetic wounds, are disclosed. The present invention includes employing a topical formulation of a beta-blocker, having substantially no antibacterial activity, to improve the process of diabetic wound healing. The present invention also involves increasing the rate of collagen accumulation of the healing epithelialized tissue in the wound of a diabetic individual.
EP0877735B1 Polycyclic compounds Compounds of Formula (I), methods for their preparation, pharmaceutical formulations and use thereof.
US7084159 Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative o thereof, wherein A, B, Ra, R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; Lck and Src kinase. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
WO2006034234A1 Crystalline form 3 of atrasentan hydrochloride Atrasentan Hydrochloride Crystalline Form 3, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed
CN101926818A Medicine composition containing tea polyphenol and alginic acid and application thereof The invention discloses a medicine composition containing tea polyphenol and alginic acid or salts thereof and application thereof. The polyphenol and alginic acid or salts thereof contained in the invention are capable of being prepared into various types of pharmaceutic preparations which comprising tablets, capsulas, granules, pills, oral solution, injection and the like. The medicine composite can be used for preparing medicines for treating and preventing peptic ulcer.
WO2011124124A1 Prasugrel hydrochloride acetic acid solvate and its crystalline, preparation method thereof Disclosed is a novel 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c] pyridine hydrochloride acetic acid solvate or its crystalline, and the preparation method of the solvate or its crystalline. The Prasugrel hydrochloride acetic acid solvate or its crystalline has better stability and solubility than Prasugrel hydrochloride. Furthermore, its pharmaceutical preparation has better dissolution and bioavailability than commercial preparation.
CN102895424A Preparation method of drug, calculus-removing powder, for treating urolithiasis The invention relates to a preparation method of a drug, calculus-removing powder, for treating urolithiasis. The method comprises the steps of drying tetrapanax papyriferus, amber, olibanum, myrrh, herba artemisiae scopariae and the like; grinding the above materials into crude powder; sub-packaging the powder in cloth bags; and decocting in water for taking. The calculus-removing powder is particularly suitable for urolithiasis resulted from urination pains or urination retention, acts fast, and has very significant curative effects. Calculus can be removed immediately after the powder is taken.
CN101028516B Medicine preparation for oral cavity An oral medicine in the form of tablet, buccal lozenge, film, or gargle for treating foul breath, periodontal abscess, pericoronitis, recurrent aphtha, etc contains the antibacterial medicine (levofloxacin and tinidazole) and menthol.
US7342017 Vanilloid Receptor 1 and metabotropic glutamate receptor 1 inhibitors; inhibition of capsaicin-induced or PH-induced activation of vanilloid receptors; antidepressant; anxiolytic agent; analgesics; addictive disorders; antiemetic agent A compound of formula: (wherein X, R1, R3, R4, and R5 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Thiadiazolylpiperazine Compound”), pharmaceutical compositions comprising a Thiadiazolylpiperazine Compound, and methods for treating or preventing, e.g., pain, depression and anxiety, in a patient comprising administering to a patient in need thereof an effective amount of a Thiadiazolylpiperazine Compound are disclosed.
CN1939325B Medicinal composition of houttuynin sodium and astragalin, its making method and usage A medical composition for preventing and treating infection and viral diseases, antipyressis, and analgesia is prepared from sodium neohouttuyfonate or its pharmacologically acceptable salt (1-20 portions) and scutelloside (30-500 portions). Its preparing process is also disclosed.
WO2011069294A1 N6-substituted adenosine derivatives, n6-substituted adenine derivatives and uses thereof The present invention provides N6-substituted adenosine derivatives, N6-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising said compounds above, and the uses of these compounds in manufacture of medicaments and health care products for sedative, hypnotics, anti-convulsion, anti-epilepsy, anti-Parkinson's disease, preventing and treating dementia.
CN101390875A New use of organic salt and inorganic salt composite solution Disclosed is a new application of organic salt and inorganic salt complex solution which has the effects of improving physical ability and prolonging the hypoxia endurance time. The inorganic salt adopts chloride salt to be added with inorganic acid salt sodium salicylate to greatly enhance the efficacies of inorganic chloride salt in improving the physical ability and prolonging the hypoxia endurance time, so as to have obvious synergistic effect between chloride salt and inorganic acid salt sodium salicylate. Animal experiments prove that inorganic chloride salt solution is continuously taken for three days to indicate exact anti-fatigue and hypoxia endurance effects. The efficacies of anti-fatigue and hypoxia endurance are greatly improved after the organic acid salt sodium salicylate is added, so as to prove that though the preparation cost of the solution is possibly increased if organic acid salt is added; the obvious synergistic effect of organic acid salt and inorganic chloride determines that the anti-fatigue ability and hypoxia endurance ability of the mixed solution of organic acid salt and inorganic chloride salt have great potential application space.
EP1990051A1 Combinations of SSRI and estrogenic agents This invention comprises methods of treating depression, anxiety, generalized anxiety disorder (GAD), hot flush, post partum depression, premenstrual syndrome, obesity, obsessive compulsive disorder, post-traumatic stress disorder, social phobia, disruptive behavior disorders, impulse control disorders, borderline personality disorder, chronic fatigue disorder, premature ejaculation, pain, attention deficit disorders, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa, or Shy Drager Syndrome comprising administration of a selective serotonin reuptake inhibitor and compound of the formula I or II: wherein Z is a moiety selected from the group of: wherein: R1 is selected frm H, OH or the C1-C12 esters or C1-C12 alkyl ehers thereof, benzyloxy, or halogen; or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or C1-C12 alkyl ethers thereof, halogens, or C1-C4 halogenated ethers, cyano, C1-C6 alkyl, or trifluoromethyl, with the proviso that, when R1 is H, R2 is not OH; Y is as defined; or a pharmaceutically acceptable salt thereof.
DE102006012871A1 Agent, useful e.g. to lower increased cholesterol levels in blood, comprises long-chain wax esters based on montana wax or its derivative and/or guerbet derivative or carnauba wax in combination with nicotinic acid Agent for the effective lowering of increased cholesterol levels in the blood, comprises long-chain wax esters based on montana waxes or their derivatives (VLCFA3: very long-chained fatty acid constituent of montana wax taking part in the fatty alcohol metabolic cycle) and/or guerbet wax derivative or the corresponding structural components of carnauba wax or shellack in combination with nicotinic acid or a prodrug form of nicotinic acid, where the long-chain carboxylic acid acids possess a chain length distribution of 14-40 carbons, preferably 28-40 carbons. - ACTIVITY : Antilipemic. - MECHANISM OF ACTION : None given.
WO2008104976A1 Amphipathic carboxylates for the treatment of immune-related disorders The present invention relates to the use of at least one long-chain optionally- substituted amphipatic carboxylates (known as MEDICA drugs) or any salt, ester or amid thereof or any combination or mixture thereof, for the treatment and prevention of immune-related disorders, particularly, inflammatory conditions. More specifically, the invention relates to particular analogs of these MEDICA drugs, the 3,3,14,14 tetramethyl-hexadecanedioic acid (Mlδbetabeta ), 4,4,15,15 tetramethyl-octadecanedioic acid (M18&ggr,-γ ) and 2,2,15,15- tetramethyl-hexadecanedioic acid (M16alphaalpha ). The invention further provides methods, oral compositions and kits for the treatment and prevention of immune-related disorders using these MEDICA drugs. The disease is any one of multiple sclerosis, neurodegenerative disease, an atherosclerotic disease, inflammatory bowel diseases, arthritis. Wherein said atheroslerotic disease is any one of cardiovascular disease, cerebrovascular disease and peripheral vessel disease, and a malignant proliferative disorder line carcinoma, myeloma, leukemia, lymphoma, sarcoma and melanoma.
US6943172 Antitumor agents; anticancer agents; sexual disorders; cardiovascular disorders Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.
CN103467560A Preparation of novel asiatic acid derivative and application thereof in antitumor drugs The invention belongs to the field of natural pharmaceutical chemistry, and relates to preparation of two new compounds 1 and 2 shown by a chemical structure general formula (I). The invention also relates to the application of the new compounds in preparation of antitumor drugs. The preparation method comprises the following steps of fermenting and cultivating the strain of absidia coerulea capable of modifying the structure of the asiatic acid screened by an inventor, converting the asiatic acid for 7-10 days, extracting the converted product by an organic solvent, separating and purifying so as to obtain the two novel derivatives of the asiatic acid.
US6858750 Such as Parkinson's syndrome, Alzheimer's disease, Huntington's disease, retinopathia pigmentosa and mitochondrial encephalomyopathy; preferred are dialkyl fumarate, monoalkyl fumarate and is salts The present invention relates to the use of individual fumaric acid derivatives or mixtures thereof for preparing a pharmaceutical composition for treating mitochondrial diseases, especially for treating Parkinson's syndrome, Alzheimer's disease, Chorea Huntington disease, retinopathia pigmentosa and mitochondrial encephalomyopathy. Preferably, the fumaric acid derivative(s) is/are those selected from the group consisting of fumaric acid dialkyl esters or fumaric acid monoalkyl esters in the form of the free acid or a salt thereof.
CN103638500A Medicament for treating diaphragmatic spasm and preparation method of medicament The invention discloses a medicament for treating diaphragmatic spasm and a preparation method of the medicament. The medicament is mainly prepared from medicines such as oldenlandia diffusa, codonopsis pilosula, persimmon calyx, flos caryophylli, rhizoma phragmitis, oyster, sword bean, azedarach and the like according to a certain weight ratio. The medicament disclosed by the invention has the functions of warming middle energizer to descend adverse-rising qi and tonifying the kidney and vitality, and is rapid to take an effect and good in curative effect when used for treating diaphragmatic spasm, and the disease is not easy to reoccur after being healed.
CN1765360A Long acting(sustained-release) amoxilin capsule and preparation method thereof Disclosed is a long acting (sustained-release) amoxilin capsule and preparation method, which comprises making amoxicillin particles or micro-pellets through conventional methods, then dressing the obtained particles or micro-pellets to make stomach- or intestine-dissolvable amoxicillin particles or micro-pellets.
CA2175429C Pharmaceutical compositions and methods Pharmaceutical compositions comprising proline, 4-hydroxyproline or a pharmaceutically acceptable salt thereof which possess antiphlogistic, antirrheumatic, analgesic and wound healing activity, and which renders them suitable for the treatment of inflammation and pain and in wound healing, and especially for the treatment of inflammatory conditions, rheumatic and non-rheumatic pain and for postoperative or posttraumatic pain, are described.
WO2012026491A1 Pluripotent stem cell cardiomyocyte differentiation-promoting agent The present invention pertains to: a differentiation-promoting agent for pluripotent stem cell cardiomyocytes that contains the compounded represented by formula (1) or a salt thereof; a method for inducing differentiation into cardiomyocytes from pluripotent stem cells; and a method for producing cardiomyocytes.
US7868205 N-[2-amino-5-(2-thienyl)phenyl]-4-{[(3,4-dimethoxyphenyl)amino]methyl}benzamide; antiproliferative, antiprotozoal agent; lymphoma, lung cancer, colon cancer, prostrate cancer, stomach cancer, breast cancer, leukemia The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
WO2006065590A3 Pyridine and pyrimidine antiviral compositions The present invention relates to pyridines and pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein, and their pharmaceutical compositions useful as antiviral compounds, and their methods of preparation and methods for use in the treatment as antiviral agents.
US8796265 Anti-infective solution comprising a compound of pyrido(3,2,1-IJ)-benzoxadiazine type An anti-infection solution including (i) from 10% to 30% by weight with respect to the total volume of the solution of at least one compound of Formula (I): wherein: X represents a hydrogen or halogen atom or a hydroxy function, R1 represents: a 1-piperazinyl radical, which may be substituted in position 4 by a methyl, acetyl or 4-aminobenzyl group; a morpholino radical: a 1-pyrrolidinyl radical substituted in position 3 by a chlorine atom or by an amino, aminomethyl, (methylamino) methyl, (ethylamino) methyl or methoxy group; a 1-imidazolyl radical that can be substituted in position 4 by the methyl group, or a 1-piperidyl radical substituted in position 4 by a hydroxy or methoxy group, and R2 represents an alkyl radical, linear, branched or ring, including 1 to 10 carbon atoms, or at least one of its pharmaceutically acceptable salts, (ii) benzyl alcohol as a stabilizing agent, and at least one stabilizing agent, and (iii) at least one solubilization agent selected from the group consisting of carbolic acids and their esters, in a pharmaceutically acceptable carrier.
WO2010080970A3 Oral enteric antidepressant formulation Pharmaceutical presentations of phenoxathiin-based MAO-A inhibitors are disclosed whereby the MAO receptors are protected from binding to active ingredient in the stomach. Particular phenoxathiin-based MAO-A inhibitors include those of the following formula: (I) wherein n is 0, 1 or 2; R1 is a branched or straight chain C1-5 alkyl or C3-6 cycloalkyl optionally substituted with hydroxyl, or one or more halogens; and X1, X2, X3, X4, and X5 are either all hydrogens or one or two of X1, X2, X3, X4, and X5 are halogen and the remainder are hydrogens, with the proviso that when n is 0 or 1 and each X is hydrogen, R1 is not methyl. A wide variety of enteric mechanisms may be utilized so as to provide release of the active ingredient essentially out of the environment of the stomach after ingestion as a pharmaceutical presentation, such as a tablet or capsule. Presentations include enteric coated tablets, enteric coated capsules, capsules containing enteric coated beads.
CN102114066A Medicinal composition for alleviating physical fatigue The invention relates to a medical configuration product, in particular to a medicinal composition for alleviating physical fatigue. The composition comprises 0.1 to 0.3 part of forest frog oviduct, 1 to 5 parts of rhodiola rosea extract, 0.1 to 0.5 part of taurine, 0.01 to 0.05 part of vitamin B1, and 0.01 to 0.05 part of vitamin B6. The composition can alleviate physical fatigue, is suitable for sportspeople, mental workers and travelers, and is particularly suitable to be drunk by highland travelers.
EP2640380A1 Pharmaceutical combination of paclitaxel and a cdk inhibitor The present invention relates to a pharmaceutical combination comprising paclitaxel, or its pharmaceutically acceptable salt; and at least one cyclin dependent kinase (CDK) inhibitor represented by a compound of formula I (as described herein) or a pharmaceutically acceptable salt thereof, for use in the treatment of triple negative breast cancer (TNBC). The present invention relates to a method for the treatment of breast cancer, particularly triple negative breast cancer, by administration to a patient in need thereof, a therapeutically effective amount of a pharmaceutical combination comprising a cytotoxic antineoplastic agent, paclitaxel, and at least one cyclin dependent kinase (CDK) inhibitor; wherein said combination on administration exhibits synergistic effects.
WO2010070023A3 Pharmaceutical orally deliverable formulations The present invention is directed to orally deliverable dosage forms with a rapid release profile comprising 4-(1,2,4,5-tetrahydro-2-oxo-3H-1,3-benzodiazepin- 3-yl)-(1 R)-1 -[(4-hydroxy-3,5-dimethylphenyl)methyl]-2-[4-(4-morpholinyl)- 1 -piperidinyl]-2-oxoethyl-1 -piperidinecarboxylate and/or a pharmaceutical acceptable salt thereof and a method for the production thereof.
US20100056585 N-(2-Aminophenyl)-4-[N-(Pyridine-3-yl)-Methoxycarbonyl-Aminomethyl]-Benzamide (MS-275) Polymorph B The crystalline Polymorph B of N-(2-aminophenyl)-4-[N-(pyridine-3-yl)methoxy-carbonyaminomethyl]benzamide (MS-275) of formula I is described, as well as the process for the production of said compound, and its use as a medicament for the treatment of selected diseases.
US20050164977 A contraceptive or hormone replacement therapy kit with at least 10 oral dosage units; preventing fetal damage, peripheral neuropathy, paresthesia or ataxia caused by vitamin B12 deficiency The present invention is concerned with a kit for use in a hormonal contraceptive method or hormone replacement therapy in mammalian females, said kit comprising at least 10 oral dosage units containing at least 1 μg of one or more steroids selected from the group consisting of estrogens and progestogens; at least 0.1 mg of one or more tetrahydrofolate components selected from the group consisting of (6S)-tetrahydrofolic acid, 5-methyl-(6S)-tetrahydrofolic acid, 5-formyl-(6S)-tetrahydrofolic acid, 10-formyl-(6R)-tetrahydrofolic acid, 5,10-methylene-(6R)-tetrahydrofolic acid, 5,10-methenyl-(6R)-tetrahydrofolic acid, 5-formimino-(6S)-tetrahydrofolic acid, pharmaceutically acceptable salts of these tetrahydrofolic acids and glutamyl derivatives of these tetrahydrofolic acids; and at least 0.1 mg vitamin B 12. Other aspects of the present invention relate to a hormonal contraceptive method and a method of hormone replacement therapy comprising the at least once daily oral administration of one or more steroid containing dosage units to a mammalian female, wherein the dosage units additionally contain at least 0.1 mg of one or more of the aforementioned tetrahydrofolate components and at least 0.1 mg vitamin B 12.
US20080097385 Therapeutic Adjuncts to Enhance the Organ Protective Effects of Postconditioning Provided herein is a method of postconditioning reperfusion of an organ or tissue injured by ischemia in combination with the administration of one or more tissue protective agents that enhance the effect of postconditioning. Also provided is a method of treating a myocardial infarction in a subject to prevent injury to the heart following reperfusion of the heart in combination with the administration of one or more tissue protective agents that enhance the effect of postconditioning.
WO2012054920A2 Antigen-specific, tolerance-inducing microparticles and uses thereof The present invention provides antigen-specific, tolerance-inducing microparticles for the targeted delivery of therapeutic agents to immune cells. In addition, the present invention allows for sustained release of therapeutic agents for a prolonged period of time. Also provided are therapeutic uses of the present invention for the prevention and/or treatment of immune diseases and autoimmune disorders. In a specific embodiment, the present invention provides treatment for type 1 diabetes.
CN103735558A Anti-variable fungi ointment, as well as preparation method and application thereof The invention provides anti-variable fungi ointment. The ointment is prepared from daktarin ointment/cream and nystatin, wherein nystatin tablets are grinded and filtered, and are then stirred with the daktarin ointment/cream to obtain the product. Daktarin has an effect of anti-variable fungi, but cannot treat root cause of the disease; nystatin cannot be absorbed by oral administration, and the effect in local application is not remarkable. The anti-variable ointment is combined by daktarin and nystatin, has a special curative effect on variable fungi, has a remarkable effect and is quick in response in tinea corporis and tinea cruris caused by variable fungi; furthermore, the skin on the focus is not influenced after fungi are eliminated.
CN101366702A Orally taken or buccal antiviral medicament-Ribavirin tablet and method of preparing the same The invention discloses an antiviral drug which can be taken orally or molten - a ribavirin tablet and a manufacturing method thereof. The compositions of the preparation by weight percent are 3.8 to 20 percent of ribavirin, 71 to 83.25 percent of sugar and 9 to 12.95 percent of other pharmaceutic adjuvant. The manufacturing method comprises the following steps: 80 meshes of the ribavirin, 80 meshes of the sugar and other filler and disintegrating agent between 80 meshes and 100 meshes are taken and mixed; an adequate bonding agent is added into the mixture and particles are prepared, boiled, dried and integrated and added with lubricant; after uniform mixture, the weight of a stator plate is tested, and tabletting is performed; and after test qualification, packaging and full inspection are performed. The preparation lightens the passivity of patients in taking medicine and particularly solves the problem of medicine taking of infants, old patients, dental patients, upper respiratory tract virus infection patients and so on; and as shown by production for a plurality of years and sampling stability study, the quality of the preparation is stable.
US20110237651 Treatment of erythropoietin (epo) related diseases by inhibition of natural antisense transcript to epo Oligonucleotide compounds modulate expression and/or function of Erythropoietin (EPO) polynucleotides and encoded products thereof. Methods for treating diseases associated with Erythropoietin (EPO) comprise administering one or more oligonucleotide compounds designed to inhibit the EPO natural antisense transcript to patients.
US20120258061 Method for Treating Skin with Retinoids and Retinoid Boosters A skin care product comprising from about 0.001% to about 10% of a retinoid in combination with 0.0001% to about 50% of at combination of retinoid hoosters.
WO2013072015A1 Morpholinyl benzotriazine for use in cancer therapy The invention relates to compounds of formula (I), where R1, L and m have the denotations as defined in the claims, and/or to the physiologically harmless salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of formula (I) can be used for inhibiting serine/threonine protein kinases and for sensitizing cancer cells to anticancer drugs and/or ionizing radiation. A further object of the invention is the use of the compounds of formula (I) in the prophylaxis, therapy or progress monitoring of cancers, tumors, metastases, or angiogenic disorders, in combination with radiotherapy and/or an anticancer drug. The invention further relates to a method for producing the compounds of formula (I) by reacting compounds of formulae (II) and (III) and, if need be, converting a chemical base or acid of the compounds of the formula (I) to one of the salts thereof.
WO2007125883A1 Composition for improvement in sleep quality Disclosed is a composition for improving the sleep quality, which has an excellent effect of improving sleep quality. The composition comprises a combination of (A) a component having an activity of enhancing a parasympathetic function and (B) a component having an activity of promoting the increase in peripheral blood flow.
CN1994303A Sustained release preparation containing pseudoephedrine and desloratadine and preparation process thereof The invention relates to a slow-release drug with pseudoephedrine and dileitadin, and relative production, wherein it is formed by slow-releaser and quick-releaser; the pseudoephedrine is slow releaser which will release 30-60% in second hour, release 50-80% in fourth hour, and 80% in eighth hour; the dileitadin is quick releaser which will release 75% in 30min. The invention will release quickly after orally intake. The invention also provides relative external releaser character and preparation.
CN101579426B Medicine for treating tinea manus and pedis The invention relates to a medicine, in particular to a medicine for treating tinea manus and pedis. The invention solves the problems that the existing medicine for treating tinea manus and pedis hashigh cost, less durable drug potency, weak penetrability and easy recurrence after medicine withdrawal. The medicine for treating tinea manus and pedis is prepared from 20 to 30 parts of keel, 4 to 7parts of membrane of hen egg, 8 to 12 parts of rhizoma coptidis from Sichuan of China, 2 to 4 parts of alum, 5 to 8 parts of dittany bark, 5 to 8 parts of rhizoma atractylodis, and 1 to 3 parts of curling factor which is oral antifungal drug. The medicine for treating tinea manus and pedis has the functions of eliminating damp toxin, relieving itching, suppressing sweat, killing epiphyte, performing constringency and strong penetrability and repairing skin barrier, and has simple formulation, reasonable compatibility, low price, safe use and no irritation to skin; the medicine enters pathopoiesia pathogenicbacteria to kill pathogenicbacteria as well as improve, dissolve and thicken horny layers, improves skin microcirculation, and restores normal structure and function of tissues; diseaseis not easy to relapse after healed, and the medicine for treating tinea manus and pedis is suitable for mycotic infection diseases of hands and feet, and has obvious healing efficacy for skin chronic diseases, such as psoriasis, neurodermitis, chronic eczema, etc.
EP1397351B1 Pyrimidine, triazine and pyrazine derivatives as glutamate receptors The present invention relates to pyrimidine, triazine and pyrazine derivatives of the general formula (I), wherein R?1, R2, R3, R4¿, X, Y and Z have the significances given in the specification ,as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing these compounds, their preparation and to their use for the control or prevention of acute and/or chronic neurological disorders.
US7186733 4-(phenyl-(piperidin-4yl)-amino)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6alkyl, NO2, CF3, C1–C6alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety or functional gastrointestinal disorders.
WO2009105430A1 Treating cancer with desthiazolyl ritonavir Treatment of cancer includes administering a compound of formula I, for example desthiazolyl ritonavir, to a subject. In particular, treatment of breast cancer is described.
US20110195980 Bicyclic Kinase Inhibitors New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
WO2014144610A1 Lactam compounds as ep4 receptor-selective agonists for use in the treatment of ep4-mediated diseases and conditions Disclosed herein are compounds of formula (I) wherein L1, L2, L3, R1, R4, R5, and R6 are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
CN102718818A Nitrogenous troxerutin derivative, preparation method thereof and application The invention discloses a nitrogenous troxerutin derivative and a preparation method thereof, and belongs to the field of medicinal chemistry. In the method, troxerutin and divinyl ester are used as raw materials, organic solvents serve as reaction media under catalysis of hydrolytic enzyme, the reaction temperature ranges from 40 DEG C to 60 DEG C, troxerutin vinyl ester is obtained and serves as a substrate respectively reacting with dimethyldiguanide or piperazine compounds under enzyme catalysis, troxerutin derivatives containing triazine rings and piperazine rings are respectively obtained, and the compounds have antitumor activity. The preparation method is moderate in reaction condition and simple in operation, the enzyme can be recycled, and a good way is provided for nitrogenous derivatization of natural products.
US7105324 Nucleic acid isolated from Tetrahymena which codes for a triterpenoid cyclase, its production, and use The present invention relates to nucleic acids isolated from Tetrahymena which code for a ciliate-specific triterpenoid cyclase. The inventive nucleotide sequences and the polypeptide sequences derived therefrom demonstrate a surprisingly minimal sequence identity to known isoprenoid cyclases. The invention also relates to the use of nucleic acids for the regulation of triterpenoid cyclase expression in a host organism, as well as the targeted knockout or repriming of the triterpenoid cyclase gene. As a result of the altered expression of the triterpenoid cyclase, it is possible to modify and enrich the levels of multiple unsaturated fatty acids in the host organism.
US20120190623 Inactivation Resistant Factor VIII The present invention provides novel purified and isolated nucleic acid sequences encoding procoagulant-active FVIII proteins. The nucleic acid sequences of the present invention encode amino acid sequences corresponding to known human FVIII sequences, wherein residue Phe309 is mutated. The nucleic acid sequences of the present invention also encode amino acid sequences corresponding to known human FVIII sequences, wherein the APC cleavage sites, Arg336 and Ile562, are mutated. The nucleic acid sequences of the present invention further encode amino acid sequences corresponding to known human FVIII sequences, wherein the B-domain is deleted, the von Willebrand factor binding site is deleted, a thrombin cleavage site is mutated, an amino acid sequence spacer is inserted between the A2- and A3-domains. Methods of producing the FVIII proteins of the invention, nucleotide sequences encoding such proteins, pharmaceutical compositions containing the nucleotide sequences or proteins, as well as methods of treating patients suffering from hemophilia, are also provided.
US20050244519 Bulking agent compositions The present invention provides an ingestible composition comprising a fibre or sacharide bulking agent, an ingestible silica, and at ingestible surfactant. The provision of the silica and the surfactant provides a synergistic benefit in the dispersal of the bulking agent in water thus making if easier and/or quicker to obtain an imbibable liquid. The bulking agent may be ispaghula, a natural material of benefit in promoting good bowel function.
CN103239398A Dammarane sapogenin suspension, and preparation method and application thereof The invention relates to a dammarane apogenin suspension, and a preparation method and an application thereof. The dammarane apogenin suspension comprises 10-60wt% of dammarane apogenin, 2-15wt% of a hydrophilic auxiliary material, phosphatides, and the balance water, wherein the weight ratio of phosphatides to the dammarane apogenin is 1:500-1:20, and the weight percentage of dammarane apogenin is 30-50%. No organic solvent is used in the preparation method of the dammarane apogenin suspension, so the residual problem of the organic solvent is avoided, and the drug loading capacity is high; the preparation method is convenient and simple, so it in benefit for the industrialized production; and the dammarane apogenin suspension is laminated to the surface of a blank pill to prepare a tablet or a capsule, so the absorption effect is good.
US7345047 7-[7-[2-cycloalkyl]amino]-5-(propylthio)--3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]spiro[2.4]heptane-4,5,6-triol from spiro[2.4]hept-5-ene-4,7diol Diacetate and 4,6-dichloro-5-nitro-3-propylthiopyrimidine intermediates; for P2T (P2Y(ADP) or P2T(AC)) receptor antagonists; antithrombotics; unstable angina The invention provides novel substituted cyclopentane compounds (in particular, substituted [1,2,3]triazolo[4,5-d]pyrimidines), their use as medicaments (in particular, their use as anti-thrombotic agents), compositions containing them and processes for their preparation.
US20100196492 Electrostatic coating of particles for drug delivery A system for electrostatically coating particles is provided. The system is particularly well suited for coating charged drug delivery particles (e.g., nanoparticles, microparticles) with a coating of opposite charge. The coating may include a targeting moiety such as a small molecule ligand, peptide, protein, aptamer, etc. The coated particles are biodegradable and/or biocompatible, have a near neutral zeta (ξ) potential, and are stable in serum. The invention also provides pharmaceutical compositions and kits including the inventive coated particles. Methods of preparing and using the inventive particles are also included.
WO2011130515A1 Arylthiazolyl piperidines and related compounds as modulators of survival motor neuron (smn) protein production Aryl substituted thiazol-2-yl-piperidines and related compounds useful as modulators of survival motor neuron (SMN) protein production are provided herein. Without being bound to any particular theory it is believed the aryl substituted thiazol-2-yl-piperidines and related compounds provided herein act to increase production of the SMN2 form of survival motor neuron protein. These compounds are useful for treating spinal muscular atrophy. Pharmaceutical compositions containing a carrier and one or more of the aryl substituted thiazol-2-yl-piperidine or related compounds described herein are also provided. Methods of treating spinal muscular atrophy are also provided by this disclosure.
CA2628534A1 Methods for inhibiting protein kinases The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim-1 kinase, and tyrosine kinase using imidazo[1,2-a]pyrazine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.
WO2009087900A1 Pharmaceutical agent for prevention or treatment of diseases accompanied by intraocular vascular hyperpermeability Disclosed is a pharmaceutical agent useful for the prevention or treatment of retinal ischemic diseases. Specifically disclosed is a pharmaceutical agent for the prevention or treatment of diseases having intraocular vascular hyperpermeability including diabetic retinopathy (simple background retinopathy, preproliferative retinopathy, proliferative retinopathy), retinal vein occlusion, retinal artery occlusion, age-related macular degeneration, central serous choroidopathy, diabetic macular edema, cystoids macular edema, uveitis and Behcet's disease. The pharmaceutical agent comprises, as an active ingredient, an angiotensin II receptor blocker such as 4-(1-hydroxy-1-methylethyl)-2-propyl-1- [2'-(1H-tetrasol-5-yl)biphenyl-4-ylmethyl]imidazole-5- carboxylic acid.
US20120202876 Methods of treating diseases with proanthocyanidin oligomers such as crofelemer Disclosed herein are methods of treating diseases including gastrointestinal disorders, such as secretory diarrheas, with the proanthocyanidin oligomer, crofelemer. Also disclosed is the anti-secretory effect of crofelemer on Calcium-activated chloride channels (CaCC) and Cystic fibrosis transmembrane conductance regulator (CFTR).
US20110206754 Implant device The present description relates to an implant device, having an improved integration in the tissue of the animal or human body into which it is inserted, when compared to the prior art devices. Particularly, the present description relates to an implant device for the implant in animal or human body, comprising a hyaluronic acid coating, characterized in that said hyaluronic acid is low molecular weight hyaluronic acid or is composed of a mixture of low molecular weight hyaluronic acid and high molecular weight hyaluronic acid, wherein said low molecular weight hyaluronic acid has a molecular weight lower than 80,000 Dalton and said high molecular weight hyaluronic acid has a molecular weight higher than 700,000 Dalton.
US20100160368 Methods of Treating Dermatological Disorders and Inducing Interferon Biosynthesis With Shorter Durations of Imiquimod Therapy Pharmaceutical Formulations and Methods for the Topical and/or transdermal delivery of imiquimod, including creams, ointments and pressure-sensitive adhesive compositions to treat dermatological disorders, namely, viral infections, such as Type I or Type II Herpes simplex infections and genital and perianal warts, actinic keratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis to achieve an antiviral effect, with shorter durations of therapy, than currently approved for imiquimod by the Food & Drug Administration (“FDA”).
CN103393683A Application of SIRT2 inhibitor in pharmacy The invention relates to the technical field of medicines, in particular to application of an SIRT2 (Sirtuin 2) inhibitor in preparation of drugs treating type 2 diabetes and drugs inhibiting insulin secretion. The acute effect test of AGK2 on rat islet glucose stimulated insulin secretion (GSIS), the test of the influence of different concentrations of AGK2 on insulin secretion, the test of the influence of AGK2 on insulin secretion under different glucose concentrations, and the test experiment of the acute effect of AGK2 on high concentration glucose induced insulin hypersecretion together prove that the SIRT2 inhibitor AGK2 can obviously inhibit glucose stimulated insulin secretion, and the AGK2 with a concentration of 0.5 micromol/l already can inhibit insulin secretion, thus providing exact experimental data for preparation of drugs treating type 2 diabetes, and also providing more scientific bases for clinically more rational use of AGK2.
WO2009044294A3 Means and methods for the treatment of cataract and presbyopia The present invention relates to an inhibitor of a protein, wherein said protein (i) comprises or consists of the amino acid sequence of SEQ ID NOs: 2 or 4, or is encoded by a nucleic acid comprising or consisting of the sequence of SEQ ID NOs: 1 or 3; (ii) comprises or consists of the amino acid sequence of SEQ ID NO: 26, or is encoded by a nucleic acid comprising or consisting of the sequence of SEQ ID NO: 25; (iii) is a fragment of the protein according to (i), or has a sequence at least 75% identical with the protein according to (i) or with said fragment of the protein according to (i), and exhibits NADPH oxidase activity; or (iv) is a fragment of the protein according to (ii) or has a sequence at least 75% identical with the protein according to (ii) or with said fragment of the protein according to (ii) and stabilizes said protein exhibiting NADPH oxidase activity; and/or an inhibitor of a nucleic acid, wherein said nucleic (v) comprises or consists of the nucleic acid sequence of SEQ ID NO: 1 or 3, or encodes a protein comprising or consisting of the sequence of SEQ ID NO: 2 or 4; (vi) comprises or consists of the nucleic acid sequence of SEQ ID NO: 25, or encodes a protein comprising or consisting of the sequence of SEQ ID NO: 26; (vii) is a fragment of the nucleic acid according to (v), or has a sequence at least 75% identical with the nucleic acid according to (v) or with said fragment of the nucleic acid according to (v), and encodes a protein exhibiting NADPH oxidase activity; or (viii) is a fragment of the nucleic acid according to (vi), or has a sequence at least 75% identical with the nucleic acid according to (vi) or with said fragment of the nucleic acid according to (vi), and encodes a protein stabilizing said protein exhibiting NADPH oxidase activity; for treatment and/or prevention of cataract and/or presbyopia. The sequences define NADPH oxidases or a subunit of an NADPH oxidase, respectively. A preferred inhibitor is a siRNA. Also provided are a method of treating cataract and presbyopia, pharmaceutical compositions, medical uses and diagnostic uses of compounds of the invention.
CN102716104A Medical organic silicon patch and preparation method thereof The invention relates to a medical patch, in particular to a medical organic silicon patch and a preparation method thereof, and belongs to the technical field of medicines. The medical organic silicon patch comprises a silicon rubber film layer, a silica gel layer and a release film, wherein the silica gel layer contains essential oil beta-cyclodextrin inclusion particles. The process of adding essential oil into a traditional organic silicon patch is changed by the preparation method of the medical organic silicon patch containing the essential oil beta-cyclodextrin inclusion particles, essential oil molecules are included into an inner cavity with beta-cyclodextrin by the aid of the beta-cyclodextrin inclusion technology, the essential oil molecules are prevented from directly contacting with platinum catalysts, being poisoned and stopping vulcanization of silica gel. According to the medical organic silicon patch prepared by the preparation method, release of active components of essential oil can be controlled by the beta-cyclodextrin and the silica gel layer in the patch, and the effects of the active components of the essential oil and double scar repair effects of silica gel are made full use of, so that scars are repaired more rapidly and effectively.
US20090062561 Deuterium-enriched latanoprost The present application describes deuterium-enriched latanoprost, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2006037347A1 Pharmaceutical compositions comprising fenofibrate and atorvastatin Pharmaceutical compositions in particulate form or in solid dosage forms comprising a combination of a reduced or low dose of fenofibrate and the HMG CoA reductase inhibitor atorvastatin or a pharmaceutically active salt thereof. Atorvastatin is optionally provided as a controlled release or a delayed release formulation, which may result in a maintained LDL-lowering effect at a reduced dosage. Fenofibrate is provided in a formulation being bioequivalent to commercially available Antara® capsules, or exhibiting increased bioavailability as compared therero, and also reduced food effect.
CN1582957A Preparation of medicines from hippophae rhamnoides for reducing blood sugar and cholesterol A medicine in the form of tablet or capsule for decreasing blood sugar and cholesterin is prepared from seabucklthorn polyose and the auxiliary chosen from microcrystalline cellulose, hydroxypropyl cellulose sodium, hydroxymethyl amylsodium and magnesium stearate.
CN103382205A Bone-targeting zinc phthalocyanine and its preparation method and use The invention discloses a bone-targeting zinc phthalocyanine and its preparation method and use. The bone-targeting zinc phthalocyanine has a structure shown in the patent specification. The bone-targeting zinc phthalocyanine (I) has good water solubility, a high cell intake amount and good biocompatibility. An in-vitro hydroxyapatite adsorption experiment and a near-infrared fluorescence living imaging and tissue imaging experiment shows that the bone-targeting zinc phthalocyanine has high bone targeting. In a near infrared area of 600-900nm, the bone-targeting zinc phthalocyanine has absorption and fluorescence effects and produces high singlet oxygen. The bone-targeting zinc phthalocyanine has wide application prospects and can be used for bone-targeting photodynamic therapy or near-infrared fluorescence imaging. The preparation method is simple and can be operated easily.
CN102488704A Preparation method of refined poly zic and application The invention provides a preparation method of refined poly zic and application, which are characterized in that polyinosinic acid and poly zic acid are purified via a chemical method, are merged into poly zic liquor after being refined respectively, and the poly zic liquor is ultra-filtered, concentrated and added with auxiliaries, so that the refined poly zic is prepared. The refined poly zic can effectively increase an anticancer effect.
US20090156684 Liquid antibacterial compositions incorporating trichlorocarbanilide with reduced water activity A liquid antibacterial soap comprising trichlorocarbanilide, wherein the composition includes, 0.1-5 wt. % trichlorocarbanilide, 0-40 wt. % water, 0.1-40 wt. % of a surfactant or mixture of surfactants, 10-60 wt. % of lower glycols to render the composition visually clear and stable, and 0.1-10 wt. % of a mixture of additional adjuvant ingredients.
WO2013013404A1 Water soluble camptothecin derivative, pharmaceutical composition and use thereof The present invention relates to a water soluble derivative of camptothecin and preparation method therefor, the derivative having a structure of formula I and being appropriate in water solubility, and having anti-cancer activity and stability of lactonic ring. The present invention also relates to a method for synthesizing the compound and medical use of the compound.
CN102895211A Sudden death and hypertension resistant metoprolol intelligent medicine release system and its preparation method The invention relates to a new medicinal preparation of a medicinal intelligent medicine release system, belongs to the biological medicine field, and concretely relates to a sudden death and hypertension resistant metoprolol intelligent medicine release system and its preparation method. The metoprolol intelligent medicine delivery system is characterized in that the metoprolol intelligent medicine release system is formed by a main controlled release layer (a tablet core, a pill core or a pellet), and the external of the main controlled release layer is coated with an intelligent film coat. Medicine release is carried out according to the human blood pressure rhythm 3-6h after the preparation is orally taken, simultaneously the main controlled release layer slowly releases medicines according to a preset medicine release speed, the highest plasma medicine concentration lasts for 10-16h, and the medicine performs the curative effect within 24h. The preparation can control the cardiogenic sudden death, the cerebral hemorrhage, the cerebral infarction and the like caused by the physiological change of the human blood pressure and the heart rate after midnight, and has very good clinical application prospects.
CN1634023A Chewing-gum for prevention and cure of stomatocace and tooth pain The invention provides a chewing gum for treating and preventing oral cavity ulcer and teeth pains, which comprises chewing gum rubber base, sweetener and perfume as the basic components, one of added borax or aldomycin or dexamethasone acetate, and several of added sodium chloride, magnesium oxide, sodium hydrogen carbonate, menthol, vitamin B1, vitamin C as adjuvant.
US20100317705 Oligomer-Dantrolene Conjugates and Related Compounds The invention relates to (among other things) oligomer-dantrolene conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
WO2005019200A3 Aryl piperidine derivatives as vla-1 integrin antagonists and uses thereof Aryl piperidine that are VLA-1 integrin antagonists are disclosed. Also disclosed are compositions containing such compounds and methods of using such compounds in treating diseases mediated, at least in part, by the VLA-I integrin.
US20060058258 Gene transcription and ionizing radiation: methods and compositions The present invention provides a DNA molecule comprising a radiation responsive enhancer-promoter operatively linked to an encoding region that encodes at least one polypeptide. An encoding region can comprise a single encoding sequence for a polypeptide or two or more encoding sequences encoding DNA binding, activation or repression domains of a transcription factor. Processes for regulating polypeptide expression and inhibiting tumor growth using such DNA molecules are also provided.
EP2676667A1 Polyethylene glycol colonic purgative composition This invention relates to novel colonic purgative compositions of polyethylene glycol having an average molecular weight of at least 1,000 or at least 4,000. Further, this invention relates to methods of using the colonic purgative compositions. The formulations and methods of this invention are particularly useful to cleanse the bowel prior to diagnostic and surgical procedures and can also be employed in lower dosages as a laxative to promote elimination and/or to relieve constipation.
EP1539136A2 Ppar alpha selective compounds for the treatment of dyslipidemia and other lipid disorders A class of benzodihydrofuran compounds having the structure of formula (I) below and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of conditions and sequelae that are associated with these diseases, such as atherosclerosis.
CN103517895A Metal-salen complex compound and production method for same The present invention provides a metal-salen complex compound comprising controlled particle diameters, in order to exhibit pharmacological effects as a medicine in a target area. The metal-salen complex compound is configured from chemicals with a crystal particle diameter of 8 [mu]m max., listed in the formula. M is Fe, Cr, Mn, Co, Ni, Mo, Ru, Rh, Pd, W, Re, Os, Ir, Pt, Nd, Sm, Eu, or Gd.
US20100069356 Dibenzothiazepine modulators of dopamine, alpha adrenergic, and serotonin receptors The present invention relates to new dibenzothiazepine modulators of D1 receptors, D2 receptors, alpha-1 adrenergic receptors, alpha-2 adrenergic receptors, H1 receptors, 5-HT1A receptors, and/or 5-HT2 receptors, pharmaceutical compositions thereof, and methods of use thereof.
US7291599 Such as amistatin and leuhistin; for control of inflammation; topical creams, gels, ointments The invention relates to a process for the treatment of neurodegenerative diseases wherein mis-folded proteins accumulate in characteristic lesions and contribute substantially to a pathogenesis and to an inflammatory reaction magnifying the damage, by the isolated or joint effect of inhibitors of the alanyl amino peptidase (APN) and of the dipeptidyl peptidase N (DP IV). Our results show that the application of inhibitors of the above-referenced enzymes or of preparations and dosage forms containing such inhibitors is definitely suitable for a therapy and prevention of dementia diseases and conditions.
US20050171105 Methods and compositions as protein kinase inhibitors The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, EGF-R, c-erbB2 kinase (HER-2), CHK2, FGFR3, p70S6K, PKC, PDGF-R, p38, TGFβ, KDR, c-Kit, b-RAF, c-RAF, FLT1 and/or FLT4 kinases.
CN102125528A Domperidone orally disintegrating tablet The invention provides a domperidone orally disintegrating tablet, which is characterized in that the tablet contains a physiologically effective amount of domperidone and a necessary pharmaceutically applicable excipient; the weight percent of domperidone in the orally disintegrating tablet is 5%-10%, and the pharmaceutically applicable excipient is a mixture of a plurality of agents selected from fillers, odor masking agents, disintegrants, surfactants, adhesives, lubricants, and glidants. The domperidone orally disintegrating tablet of the invention has the advantages of quick disintegration, excellent mouthfeel, stable quality, and reliable curative effects, and can improve the compliance of medicine taking for patients.
CA2601558A1 Method of treating cancer by administration of 5-substituted nucleosides The invention relates to methods of administration of at least one overexpression inhibitor of DNA repair genes and/or oncogenes (e.g., (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU), or a prodrug, or salt thereof) to increase the cytotoxic effect of a cytostatic or cytotoxic chemotherapeutic agent during and/or after chemotherapy, e.g., in the treatment of cancer.
EP1311241B1 Use of a porous carrier A porous carrier having interconnected porosity is loaded with drug or other material for controlled release of the drug or other material.
WO2014071000A1 Class of hdac inhibitors expands the renal progenitor cells population and improves the rate of recovery from acute kidney injury Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.
US20100008986 Pharmaceutical compositions comprising sumatriptan and naproxen The present invention relates to the pharmaceutical composition comprising sumatriptan succinate and naproxen sodium, with a proviso that both the active components are in admixture with each other.
CN102091037A Preparation method and application of liposomes of shikonin and derivatives or modifiers thereof The invention belongs to the fields of pharmaceutical engineering and biotechnology, particularly relates to a prescription process for preparing a shikonin liposome and an effect of the shikonin liposome on resisting generation of new blood vessels. A human umbilical vein endothelial cell (HUVEC) strain is adopted in an anti-angiogenic test, and inhibition (MTT) on a proliferation effect thereof and inhibition (Transwell) on a migration effect thereof are measured. In addition, the invention also relates to shikonin cysts in liposomes, bright red fluorescent light can be observed under the excitation of green fluorescent light, and the shikonin cysts have important application values in the aspects of encapsulation rate measurement, in-vitro cellular localization, endocytosis mechanisms, in-vivo drug tracking and the like. After the shikonin liposomes act on the HUVEC or other tumor cells for a period of time, a confocal microscopy can be used for carrying out cellular fluorescent localization.
US7067520 Antidiabetic agents; hypoglycemic agents; antilipemic agents; dietetics The present invention provides a preventive or therapeutic medicine for diabetes containing as an active ingredient a fused-heterocyclic compound of the formula (I′) or its salt: [wherein G is CN, NO2, CO2R4, CHO, SO2NRaRb or CONRaRb; R1 is a halogen atom, a —O—R5 group or a —S—R5 group; R2 is a halogen atom, a —O—R5 group (wherein R5 is as defined above) or an amino group which may be substituted; and each of R8 and R10 which are independent of each other, is a hydrogen atom, a halogen atom or an alkyl group].
CN1861086A Pirarubicin emulsion composition A composite theprubicine emulsion of oil-in-water type is prepared from theprubicine, oily carrier, water and surfactant. Its preparing process is also disclosed.
EP2086549A1 Therapeutic combination of a panher/vegfr2 kinase inhibitor and a platinum compound This invention relates to a synergistic therapeutic combination of anti-cancer compounds which comprises a) a panHER/VEGFR2 kinase inhibitor, and b) a platinum compound, and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use. The invention also relates to treating certain cancers utilizing the combination of the invention.
EP0506830B1 Uncharged morpholino-based polymers having phosphorous-containing chiral intersubunit linkages A polymer composition is disclosed composed of morpholino subunit structures linked together by uncharged, phosphorous-containing chiral linkages, one to three atoms in length. These chiral linkages join the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-pairing moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide.
WO2007020509A1 Combination of methylol transfer agents with tumour-inhibiting proteins or peptides and the use thereof for the treatment of cancer or tumor growth Pharmaceutical combinations and methods of treatment are provided for treating, preventing, inhibiting or reducing cancer or tumor growth in a subject utilizing a cancer or tumor-inhibiting methylol transfer agent and a cancer or tumor- inhibiting protein or peptide which includes a cancer or tumor-inhibiting multiple target inhibitor, a cancer or tumor-inhibiting tyrosine kinase inhibitor, a cancer or tumor-inhibiting small molecule inhibitor, a cancer or tumor-inhibiting small molecule, a cancer or tumor-inhibiting antibody or a combination thereof. The methylol transfer agent and protein or peptide can be administered separately or together.
CA2795923A1 Tapentadol for use in the treatment of irritable bowel syndrome The invention relates to tapentadol for use in the treatment of Irritable Bowel Syndrome.
WO2011133673A1 Use of bis [thiohydrazide amide] compounds such as elesclomol for treating cancers Improved cancer treatments with bis [thiohydrazide amide] compounds such as elesclomol, in particular for identifying patient populations that would benefit from such treatments.
US20100267652 Method of inhibiting abcg2 and related treatments Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2 or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering peliomycin and other compounds described herein.
US20080269185 Administering an oxygen scavenger; superoxidase dismutase minetic Methods and kits for treating oral mucositis are disclosed. The treatment comprises administering to a patient in need thereof a Reactive Oxygen Species scavenger in a pharmaceutically acceptable formulation.
US20120121724 Film comprising therapeutic agents The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin, as well as other therapeutic agents either with or without nitroglycerin, through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.
CN102993192A Oxazolidinone compound as well as preparation method and application thereof The invention discloses an oxazolidinone compound as well as a preparation method and an application thereof. The oxazolidinone compound is a compound shown as a formula (I-I), a formula (I-II) or a formula (I-III) or pharmaceutically acceptable salts thereof. According to the oxazolidinone compound as well as the preparation method and the application thereof, pseudouridine is led into one end of a molecule of a linezolid antibiotic to obviously improve the activity of the linezolid antibiotic.
CN103070819A Method for preparing tulathromycin oral paste The invention relates to a tulathromycin oral paste used for treating animal respiratory diseases. Besides a preservative and a wetting agent, the paste comprises an active substance with a weight accounting for 0.1-20% and a particle size of 1-10mum. The balance of the oral paste is composed of water with which the weight is added to 100%.
EP2143341A1 Nutritional Composition Containing Oligosaccharide Mixture A nutritional composition for administration to an infant which composition comprises, on a dry matter basis, from 2.5 to 15.0 wt% of an oligosaccharide mixture consisting of N-acetylated oligosaccharide(s), galacto-oligosaccharide(s) and sialylated oligosaccharide(s) with the proviso that the composition comprises at least 0.02 wt% of an N-acetylated oligosaccharide, at least 2.0 wt% of a galacto-oligosaccharide and at least 0.04 wt% of a sialylated oligosaccharide and that the N-acetylated oligosaccharide(s) comprise 0.5 to 4.0% of the oligosaccharide mixture, the galacto-oligosaccharide(s) comprise 92.0 to 98.5% of the oligosaccharide mixture and the sialylated oligosaccharide(s) comprise 1.0 to 4.0% of the oligosaccharide mixture. The composition is useful for administration to an infant in the first six months of life to reduce the risk of obesity later in life.
WO2008058288A3 Sustained release methotrexate formulations and methods of use thereof Described herein are methods of treating a disease by treatment with oral sustained release methotrexate alone or in combination with folates. In some embodiments, these approaches improve the pharmacotherapeutic performance of methotrexate therapy. Described herein are novel pharmaceutical compositions for oral administration. Also described herein are novel pharmaceutical compositions for the controlled, sustained delivery of one or more drugs to the stomach or upper gastrointestinal tract. Further described are novel pharmaceutical compositions with increased gastrointestinal residence time. More particularly, novel pharmaceutical compositions which can simultaneously, float in gastric fluid, adhere to the mucosal surfaces of the gastrointestinal tract, swell to a size which delays passage through the pylorus, are described herein. In some embodiments, the pharmaceutical compositions comprise methotrexate. In some embodiments, the pharmaceutical compositions comprise methotrexate and a folate compound. Also described herein are methods for treating or preventing diseases, by administration of the pharmaceutical compositions described herein.
US20090270472 Method to use oxymetazoline to interrupt the development of the common cold syndrome This invention describes a new manner of treating the common cold. It claims that treatment with Oxymetazoline nasal spray at the time of onset of first cold symptom(s) can interrupt the development of the common cold syndrome and result in cure of the cold.
WO2010023170A1 Dosage form comprising 1-isopropyl-4-{[4-(tetrahydro-2H-pyran- 4-yloxy)phenyl]carbonyl}hexahydro-1H-1,4-diazepine or a salt thereof The invention relates to a dosage form for oral administration comprising a carrier tablet, wherein the carrier tablet is at least partially (preferably partially) covered by a film comprising 1-isopropyl-4-{[4-(tetrahydro-2H-pyran-4- yloxy)phenyl]carbonyl}hexahydro-1H-1,4-diazepine (formula I) or a pharmaceutically acceptable salt thereof, such as the mono-maleate salt thereof. In particular embodiments, the film, which at least partially covers the carrier tablet, comprises a stabiliser (e.g. citric acid), and/or a film former (e.g. hydroxypropylcellulose). The film is preferably present in a recess on the carrier tablet. The invention also relates to a method of producing said dosage form.
WO2013143259A1 Phosphodiesterase-4 inhibitor capable of avoiding vomit reaction and preparation method for same The present invention relates to a phosphodiesterase-4 inhibitor capable of avoiding a vomit reaction. The phosphodiesterase-4 inhibitor is a compound, a prodrug or a solvate represented by DTPM. The name of DTPM is 1-(4-difluoro methoxy-3-(tetrahydrofuran-3-oxyl)phenyl)-3-dimethyl-1-ketone, and a chemical formula is shown in formula (I). The compound in the present invention can prepare a drug that can effectively weaken or even avoid an adverse reaction such as vomit, can treat depression and alzheimer disease and can improve cognitive competence.
US20110190311 Use of cdk inhibitor for the treatment of glioma The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.
EP1524263A1 prodrugs containing cycloalkene derivatives The present invention provides a prodrug of a compound represented by the formula: wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula: wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents,
CA2196656C Method for the preparation of (±)-calanolide a and intermediates thereof A method of preparing (~)-calanolide A, (1), a potent HIV reverse transcriptase inhibitor, from chromene (4) is provided. Useful intermediates for preparing (~)-calanolide A and its derivatives are also provided. According to the disclosed method, chromene (4) intermediate was reacted with acetaldehyde diethyl acetal or paraldehyde in the presence of an acid catalyst with heating, or a two-step reaction including an aldol reaction with acetaldehyde and cyclization either under acidic conditions or neutral Mitsunobu conditions, to produce chromanone (7). Reduction of chromamone (7) with sodium borohydride, in the presence of cerium trichloride, produced (~) (~)-calanolide A. A method for resolving (~)-calanolide A into its optically active forms by a chiral HPLC system or by enzymatic acylation and hydrolysis is also disclosed. Finally, a method for heating or preventing viral infections using (~)-calanolide or (-)-calanolide is provided.
EP1862462A1 Process for the preparation of desloratadine The present invention relates to an improved process for the preparation of Form 1 of desloratadine essentially free of Form 2. The invention also relates to Form 1 of desloratadine substantially free of Form 2, process for its preparation, pharmaceutical composition comprising it and its method of use for the treatment of allergic reactions in mammals.
US20090286780 2-oxochromene derivatives To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.
WO2013096684A1 Hypoxia activated prodrugs and mtor inhibitors for treating cancer Cancer is treated by administration of a hypoxia activated prodrug in combination with an mTOR inhibitor.
US20120329815 Famciclovir for the Treatment of Recurrent Herpes Labialis using a One-Day Treatment A method for the treatment of recurrent herpes labialis in mammals, including humans, which method comprises administering to the mammal in need of such treatment, and effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a period of one day.
WO2011014872A2 Compositions and methods for diagnosing, treating or preventing neoplasias As described below, the present invention features compositions and methods for diagnosing, treating and preventing neoplasias.
CN101214240A Application of indole-2, 3-diketone in preparing antiphlogistic medicament The present invention relates to an application of indole-2, 3-dione for preparing for an anti-inflammation drug. The indole-2, 3-dione is natural product or synthetic product with low toxicity, little side effect and good anti-inflammation and diminishing inflammation effects.
WO2012059725A8 Peg or peg block copolymers for treating colorectal cancer The present invention relates to methods for and of treating, ameliorating or preventing colorectal cancer (CRC) in humans using polyethylene glycol (PEG) or a PEG block-copolymer such as Pluronic® F68. Compositions for use in treating, ameliorating and/or preventing CRC comprising PEG are also disclosed. Such compositions may be used in the methods of the invention.
CN101336910A Chlorhexidine composition with colouring function The invention relates to a hibitane composition with coloring function, which comprises hibitane or a pharmaceutically-acceptable salt thereof and at least one coloring agent. The inventive composition also comprises a pharmaceutically-acceptable carrier.
CN101549158A Sodium alginate liver-targeted nanometer drug delivery system and preparing method thereof A sodium alginate liver-targeted nanometer drug delivery system uses sodium alginate as carrier material and uses glycyrrhetic acid as liver-targeted compound. The single-end-modified glycyrrhetic acid-ethylene diamine is prepared through the reacting between the carboxy group of glycyrrhetic acid and the ethylene diamine. The glycyrrhetic acid-sodium alginate is prepared through the reacting between the carboxy group of sodium alginate and the amino group of glycyrrhetic acid-ethylene diamine. Finally the sodium alginate liver-targeted drug delivery nanometer particles are prepared through crosslinking the glycyrrhetic acid-sodium alginate through calcium ions. The invention has a beneficial effect that the liver-targeted nanometer drug delivery system prepared by the invention has high liver targeting property. The hydrophilic anticancer drug and hydrophobic anticancer drug can be packaged simultaneously or a single anticancer drug is packaged. The sodium alginate liver-targeted nanometer drug delivery system of the invention has the advantages of sustained-releasing function of drug, reduced drug dosage, reduced drug taking times, reduced toxic-side effect of drug, increased drug effect, simple and practical preparing method, and excellent application prospect.
US7265115 Central nervous system-active cholinergic ligands for neuronal nicotinic receptors; Controlling synaptic transmission; selectively controlling neurotransmitter release; a (halopyridazinyl)-3,8-diazabicyclo(3.2.1)octane Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.
DE102012018789A1 New N-isopropylcarbamate compound is phospholipase A2 inhibitor, useful for prophylactic and/or therapeutic treatment of diseases e.g. inflammation, psoriasis, cerebral ischemia, Alzheimer's disease, chronic skin diseases and thrombosis N-isopropylcarbamate compound (I) or its enantiomers, diastereomers and salts and/or esters is new. N-isopropylcarbamate compound of formula (I) or its enantiomers, diastereomers and salts and/or esters is new. Q : R1, OR1 or SR1; R1 : aryl (substituted with 1 or 2 substituents of R2), linear 1-16C-alkyl, linear 2-16C-alkenyl or linear alkynyl (all substituted with O, S or aryl and interrupted with 1-6C-alkyl) or H; R2 : 1-6C-alkyl, halo, OR8, SR8, NO 2 or CF 3; Ar1 : aryl substituted with 1 or 2 substituents of R2; either R3, R5 : H; R3+R4+C, R4+R5+C : benzene ring (substituted with R6 substituent and substituted with R2 substituent), provided that when R5 is H, then R3+R4+C is benzene ring and when R3 is H, then R4+R5+C is benzene ring; R6 : COOH or CONR7R8; R7 : H, 1-6C-alkyl or aryl; R8 : H or 1-6C-alkyl; R9 : OR10 or SR10. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Antiinflammatory; Analgesic; Antipyretic; Antiallergic; Antiasthmatic; Antipsoriatic; Cerebroprotective; Vasotropic; Neuroprotective; Nootropic; Dermatological; Antirheumatic; Prevention: Anticoagulant / Treatment: Thrombolytic; Immunosuppressive; Antibacterial; Cytostatic. MECHANISM OF ACTION : Phospholipase A2 inhibitor.
CN1887717A Nanometer binary anticancer RE compound and its prepn and application The present invention relates to nanometer binary anticancer RE compound and its preparation process. The compound has the chemical expression of RE(A)2, RE is one or more RE ions selected from La3+, Ce3+, Pr3+, Nd3+, Sm3+, Eu3+, Er3+ and Y3+, and A is molybdate radical or tungstate radical. The nanometer binary anticancer RE compound of the present invention has simple preparation process, low cost, high anticancer capacity, small dosage, low toxicity, environment friendship and important anticancer application foreground.
CN102558277A Synthesis method of titerpene saponin compound stryphnoside A The invention relates to a synthesis method of a titerpene saponin compound, belonging to the technical field of organic chemistry. Stryphnoside A molecule is synthesized by using a 'convergent' synthesis strategy and applying a multi-step selective coupling method, and shows remarkable biological activity on the aspects of cancer prevention, diabetes suppression and the like.
CN102349924A Centella asiatica triterpenic acid single-glucopyranoside composition, its preparation method, its quantitative analysis method and its application The invention relates to a centella asiatica triterpenic acid single-glucopyranoside composition which is composed of ursane madecassic acid single-glucopyranoside, madecassic acid single-glucopyranoside and oleanane chebuloside II, wherein the mass ratio of ursane madecassic acid single-glucopyranoside to madecassic acid single-glucopyranoside to oleanane chebuloside II is 1:0.5-2:0.1-1, and the sum of the mass percentage content of three components is not less than 50%. The composition takes a centella asiatica extract as a substrate, the centella asiatica extract is fermented and hydrolyzed by microbes of beta-glucosidase or microbes capable of generating beta-glucosidase, and extracted by n-butanol or separated and purified by macroporous adsorption resin. The invention also provides a quantitative analysis method which is a HPLC quantitative analysis for three components by adding a proper amount of mobile phase of beta-cyclodextrin. Experimental research of pharmacodynamics proves that the composition has substantial activity for inhibiting tumor cells and fibroblast, the composition can be used for treating tumor and scar hyperplasia.
CN1977902A Injection total saponins of paeonia powder without additive material The present invention relates to a red peony total glycoside powder injection preparation containing any additive auxiliary material so as to raise stability and safety of said injection preparation. The described red peony total glycoside is any one of glycoside components obtained by extracting paeonia lactiflora pall. Or paeonia veitchii lynch or combination of arbitrary several kinds. In the invented red peony total glycoside powder injection preparation the red peony total glycoside content is 80-99.9%, in which the paeoniflorin content is 70-99.9%. Besides, it also contains small quantity of benzoic acid, paenol and water. Said powder injection preparation has the effect for resisting thrombosis, and can be used for curing the diseases of cerebral thrombotic infarct, etc.
US20090076025 Deuterium-enriched dasatinib The present application describes deuterium-enriched dasatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN103191067A Freeze-dried powder injection of bromhexine hydrochloride and preparation method thereof The invention relates to the field of pharmaceutical preparations, and in particular relates to freeze-dried powder injection of bromhexine hydrochloride and a preparation method thereof. The freeze-dried powder injection of bromhexine hydrochloride is prepared from bromhexine hydrochloride, acidity regulator, pharmaceutically acceptable accessories and water for injection; and the acidity regulator is one or more than two of benzoic acid, citric acid, acetic acid, malic acid, boric acid, phosphoric acid and lactic acid. According to the invention, the stability of the preparation is improved; the bioavailability is high; oxidative degradation can be effectively prevented; reactions such as nausea and stomach discomfort, caused by oral medicines, are avoided; and the freeze-dried powder injection of bromhexine hydrochloride disclosed by the invention is conveniently used in clinical.
WO2008046242A1 The novel quinazoline derivatives,preparation methods and uses thereof A kind of novel quinazoline derivatives represented by the general formula (I), their pharmaceutically acceptable salts, hydrates, solvates, polycrystals or eutectic crystals, their precursors or derivatives which have the similar biological functions, their preparation methods and the compositions comprising one or more present compounds are disclosed. The present application also discloses the uses of present compounds which have the antiproliferative activities, for the manufacture of pharmaceutical medicaments for the treatment of relative diseases, such as anticancer.
CN103613600A Anilino podophyllotoxin derivative with anti-tumor activity and preparation method and application thereof The invention discloses an anilino-substituted podophyllotoxin derivative with anti-tumor activity and a preparation method and application thereof. According to the method, 4-chloro-3-methylaniline, 3-fluoro-4-methoxyaniline, 4,4'-diamino diphenylmethane, ortho aminoanisole, 4-chloro-2-aminoanisole, ortho-anthranilo nitrile, 2,6-dichloro-4-aminophenol, N,N-dimethylamino meta-aniline, 2-ethyl-5-nitroaniline, 2,2'-diaminodiphenyl thioether or 2-aminobenzotrifluoride are respectively introduced to an activated C-ring fourth position of a podophyllotoxin or 4'-demethyl epipodophyllotoxin through an anilino reaction, so as to obtain the anilino-substituted podophyllotoxin derivative represented by a formula (V) shown in a drawing. The derivative disclosed by the invention acts on tumor cells through multiple ways and multiple target points, the anti-tumor activity is remarkably improved, and the derivative can be used for preparing anti-tumor drugs and is applied to clinical anti-tumor treatment.
US20090175845 Methods for identifying compounds that modulate phb domain protein activity and compositions thereof The invention relates to the finding that PHB domain polypeptides can bind cholesterol and related compounds and are involved in the regulation of various cellular activities. Accordingly, the invention includes methods of identifying compounds that can bind to and/or modulate activity of a PHB domain polypeptide such as Podocin or MEC2.
CN103202855A Medicament composition for preventing and curing newly-born piglet diarrhea syndrome The invention discloses a medicament composition for preventing and curing newly-born piglet diarrhea syndrome, a preparation method of the medicament composition and application of the medicament composition to preventing and curing of newly-born piglet diarrhea syndrome, belonging to the field of veterinary medicaments. The medicament composition comprises kalii dehydrographolidi succinas, berberine hydrochloride, nano montmorillonite powder, glucose, sucrose and dextrin. The medicament composition can eliminate and restore pathological injuries of newly-born piglet diarrhea syndrome, has the functions of broad spectrum antivirus, antisepsis and anti-inflammation, and is capable of restoring and improving the defense of a digestive tract mucosa barrier to attack factors, improving the regeneration of injured digestive tract mucous epithelium, relieving a hypoglycemia symptom, maintaining the normal physical functions of a digestive tract, preventing and relieving newly-born piglet diarrhea syndrome caused by multiple reasons, and reducing the morbidity of newly-born piglets. The compound veterinary medicament linctus provided by the invention is applied to newly-born piglet diarrhea syndrome in a simple and easy dosage form and administration route, is obvious in curative effect, low in stress, non-toxic, harmless and free of residue, and conforms to large-scale cultivation production requirements.
US20110230488 Hybrid-ionone and curcumin molecules as anticancer agents The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesised and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breast cancer and lung cancer cell lines.
CN102557983A (4-substituted benzoyl) fluorobenzene salicylamide compound and application thereof The invention discloses (4-substituted benzoyl) fluorobenzene salicylamide compound shown in a formula (II) and discloses an application of the (4-substituted benzoyl) fluorobenzene salicylamide compound to preparing anti-tumor drugs, especially anti-endometrial-cancer drugs. The invention has the beneficial effects of: (1) providing a preparation method of the (4-substituted benzoyl) fluorobenzene salicylamide compound; (2) providing a new anti-endometrial-cancer drug with obvious anti-tumor activity, providing research basis for new-drug screening, and having a great application prospect; and (3) being simple in preparation process and being beneficial to industrial production.
US20120070510 Wound and mucous membrane disinfectant Aqueous wound and mucous membrane disinfectant containing a) octenidine dihydrochloride, and b) one or more active ingredients selected from the group ethanol, 1-propanol, 2-propanol, undecylene amidopropyl trimonium methosulfate, 3-(4-chlorophenoxy)-1,2-propanediol and/or sodium hydroxymethylglycinate and c) glycerin and/or 1,2-diols having 3 to 10 carbon atoms, and d) optionally surfactants, emulsifiers, solubilisers, pH regulators, dyestuffs, perfumes and/or thickeners, the agent being free of phenoxyethanol, phenoxypropanol, phenoxyisopropanol and organic acids.
CN101787116A Compound and application thereof in preparing drug for curing viral respiratory infection The invention belongs to the field of pharmacy, disclosing a compound and application thereof in preparing a drug for curing viral respiratory infection. The compound comprises the following structural formula shown in a formula (I), wherein R is-CH2-CH2-, R' is linear chain or multiple-chain alkyl of C4-C14, x is 1-50, and y is 0-50. The compound has the effect of resisting respiratory system viral infection and can be used for preparing the drug for treating respiratory system viral infection.
US20100087386 Topical use of levofloxacin for reducing lung inflammation The present invention relates to methods and compositions for the treatment of pulmonary inflammation. In particular, methods and compositions using aerosol levofloxacin or ofloxacin to reduce pulmonary inflammation are provided.
CN101606914A Cefuroxime axetil tablet preparation suitable for direct powder compression The invention provides a cefuroxime axetil tablet preparation suitable for direct powder compression, and the preparation comprises the following compositions by weight ratio: 50-70% of cefuroxime axetil, 20-40% of a filler, 0.5-1% of a glidant, 5-15% of a disintegrant and 1-3% of a surfactant; and all compositions of the preparation are powder, and appropriate weight of each tablet is 450-600mg. By selecting suitable adjuvants, the preparation is ensured rapid disintegration and leaching of the tablet and solves a problem that direct powder compression technique is not suitable due to low density and poor fluidity of the shapeless cefuroxime axetil and difficulty in filling on a common tablet press. In the preparation, bulk density of microcrystalline cellulose is about 0.4g/cm, and the bulk density of the disintegrant is greater than 0.35%, which causes mixed powder containing the shapeless cefuroxime axetil to have the density up to 0.3g/cm, and compressibility and filling properties to be suitable for requirements of direct compression.
CA2559439A1 Compositions for inhibiting or reducing inflammation of skin The invention features a composition and methods for treating inflammation of skin, where the composition contains hydrocortisone and an avenanthramide.
WO2007142297A1 Composition for prevention/treatment of hepatic disease Disclosed are a composition for prevention and/or treatment of hepatic diseases and a composition for prevention and/or treatment of diseases associated with insulin resistance. The compositions contain a component selected from the group consisting of asparagines, salts thereof and mixtures of them as an active ingredient.
US20090076019 Methods for treating neurological disorders or damage A clonogenic neurosphere assay is described that carries out high throughput screens (HTS) to identify potent and/or selective modulators of proliferation, differentiation and/or renewal of neural precursor cells, neural progenitor cells and/or self-renewing and multipotent neural stem cells (NSCs). Compositions comprising the identified modulators and methods of using the modulators and compositions, in particular to treat neurological disorders (e.g. brain or CNS cancer) or damage are also disclosed.
CA2551578A1 Lignan complex derived from flax seed used for treatment of hypercholesterolemic atherosclerosis A method of treating hypercholesterolemic atherosclerosis in a mammal exhibiting symptoms of the disease. The method comprises administering to the mammal an effective amount of a lignan complex derived from flax and containing about 34 to 38% by weight of secoisolariciresinol diglucoside. The invention also relates to compositions and uses of the complex suitable for the treatment of the disease and related conditions.
CN102250142A Andrographolide compound and application of andrographolide compound in medicaments The invention relates to an andrographolide derivative the structure of which is shown in a formula (I) or (II) and a stereoisomer, a stereomer, a tautomer, a solvate, a polymorph, a metabolin, ester, a pharmaceutically acceptable salt or a prodrug of the derivative. The andrographolide compound provided by the invention has the advantages of good solubility, high purity and good antipyretic property; and the andrographolide compound is especially suitable to be used as an effective component for preparing antipyretic, anti-inflammatory and antimicrobial medicaments.
WO2012168664A1 4-{3-[trans-hexahydrocyclopenta[c]pyrrol-2(1h)-yl]propoxy}benzamide, method for preparing same and pharmaceutical compositions that contain same The invention relates to 4-{3-[trans-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide and the enantiomers thereof, as well as to the pharmaceutically acceptable acid or base addition salts thereof.
WO2012149528A1 Inhibitors of inducible form of 6-phosphofructose-2-kinase The invention is directed to inhibitors of inducible form of 6-phosphofructose-2-kinase of formula I, as well as to pharmaceutically acceptable salts of formula I, and pharmaceutical compositions comprising a compound of formula I. The compounds can be used to treat cancer.
WO2013050341A1 Azabenzoxazine derivatives as crac modulators Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with calcium release-activated calcium channels (CRAC).
US20100260850 Controlled Release Devices and Methods for Delivery of Nucleic Acids Embodiments of the invention include devices and methods for the delivery of nucleic acids. In an embodiment the invention includes a controlled release device including a polymeric matrix and a nucleic acid delivery construct disposed within the polymeric matrix. The nucleic acid delivery construct can include a nucleic acid molecule and a peptide molecule. The nucleic acid delivery construct can be configured to exhibit elution properties of a peptide from the polymeric matrix. The polymeric matrix can be configured to elute the nucleic acid delivery construct. Other embodiments are included herein.
US7393837 Method for treating metabolic bone disease such as osteomalacia and osteoporosis in a patient by administering a compound that modulates phosphate regulating endopeptidase homolog (PEX) expression and/or PEX enzymatic activity The present invention relates to a method of treating metabolic bone diseases in a patient, which comprises the modulation of PEX activity to modulate the bone micro-environmental concentrations of critical bone anabolic agents, namely PTH and PTHrP. The present invention also provides the use Of inhibitors of PEX activity, such as, the use of inhibitors of NEP and/or ECE and/or PEX such as phosphoramidon, and analogs thereof, to modulate and preferably increase PTH/PTHrP levels in bone microenvironment to consequently result in an increase in bone formation, as confirmed by serum bone markers, namely, osteocalcin, to thereby provide a novel method for treating metabolic bone diseases, such as osteomalacia, osteoporosis, osteopetrosis, Paget's disease and X-linked hypophosphatemic rickets.
US20100130544 Use of parasympatholytic substances to enhance and accelerate stem cell differentiation, related methods and compositions The invention refers to the in vitro and in vivo use of parasympatholytic substances, preferably scopolamine, to potentiate and accelerate the differentiation of stem cells into cells with a tissue-specific phenotype, and the process and compositions related thereto.
EP2408767A2 Amide derivatives as neuropeptide y5 receptor ligands Disclosed are a series of neuropeptide Y Y5 receptor ligands, and as such are useful to treat disorders related to mood, stress, ADHD, cognition, stress and dementia.
WO2013048965A1 Methods for treatment of diseases The present disclosure relates to methods of treating a range of diseases or conditions. The methods involve administration of a superoxide dismutase mimetic
US7547686 Combretastatin A-3 prodrug A new and more efficient synthesis of combretastatin A-3 (2a) was completed (8.4% overall yield) starting from methyl gallate and isovanillin with aldehyde 5 and phosphonium salt 8 as key intermediates. Conversion of combretastatin A-3 (2a) to a series of diphosphate prodrugs (lOa-lOl) containing selected anions was achieved. Both the diphosphate sodium (lOa) and potassium salts (lOc) displayed aqueous solubility in excess of 220 mg/ml at room temperature and good cancer cell line inhibitory activity.
WO2013160492A1 Combination therapy for the treatment of metabolic diseases The invention relates to the use of beta-3 adrenergic receptor agonists in a combination therapy for the treatment of metabolic diseases, such as hyperglycemia, insulin resistance, type 2 diabetes, and dyslipidemia. This therapy combines the administration of a beta-3 adrenergic receptor agonist with a GLP-1 receptor agonist or a PPARα agonist, both compounds being capable of reducing appetite, reducing weight gain and increasing energy expenditure by means of fat mobilisation. The invention demonstrates that the combined administration of said compounds has a synergistic effect on the reduction of body fat.
WO2008152142A1 2 -aminoquinazoline derivatives and their therapeutic uses A compound of formula (I) wherein X is NH2or OH and W is -C(O)-O- or -O-C(O)-; use thereof as a medicament, in particular for the treatment of inflammation, autoimmune disorder, immunogenic rejection reactions and cancer and for non-surgical abortion.
CN103570721A Triazolopyrazine(one) and isoxazolopiperidone compounds The present invention discloses a class of triazolopyrazine(one) and isoxazolopiperidone compounds, preparation methods, drug compositions, and uses thereof. The three classes of the compounds can adopt intramolecular 3+2 cycloaddition reactions and other necessary steps to prepare heterocyclic compounds. The compounds provide inhibition effects for heat shock protein 90 (Hsp90) so as to be used for malignant tumor treatments, particularly for treatments of melanoma, gastric cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermal carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer, and colon cancer.
WO2010068708A3 3'-azido purine nucleotide prodrugs for treatment of viral infections The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, and HBV, in human patients or other animal hosts. The compounds are 3'-azido-2',3'-dideoxy purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1 and HBV.
CN102525877A Preparation of butoconazole nitrate in-situ gel The invention relates to the technical field of medicines, in particular to a formulation for external use, namely a gel of an antifungal medicine butoconazole nitrate and a preparation process for the gel. The butoconazole nitrate is a commonly used clinical medicine; and the conventional formulation is mainly cream. The gel is prepared by taking the butoconazole nitrate as a main medicine and adding different excipients, and the medicine concentration at the local affected part is improved through dermal or mucosal administration, so that the effective inhibitory concentration is quickly achieved, and the therapeutic effect is quickly exerted. Compared with the conventional product, the invention has the advantages that: the obtained butoconazole nitrate in-situ gel has stable properties and is convenient to use; and moreover, the antibacterial effect of the butoconazole nitrate is also improved.
WO2009072629A1 Skin external preparation [PROBLEMS] To provide a skin external preparation which is capable of sustainedly releasing a fat-soluble drug (retinol, tocopherol acetate, etc.) while controlling the initial penetration speed and thereof and, therefore, shows reduced skin irritation, a refreshing texture, a high safety and a high stability. [MEANS FOR SOLVING PROBLEMS] A skin external preparation containing a fat-soluble drug-containing wax microdispersion composition, wherein the fat-soluble drug-containing wax microdispersion composition comprises a solid or semisolid wax, a nonionic surfactant, an aqueous dispersion medium and a fat-soluble drug, the ratio by mass ofthe nonionic surfactant/the wax is 1.0 or more, and the wax containing the fat-soluble drug enclosed therein is finely dispersed in a solid or semisolid state in the aqueous dispersion medium.
US7267822 Cytomodulating lipophilic peptides for modulating immune system activity and inhibiting inflammation Novel oligonucleotides comprising a sequence derived by a computer program are provided for inhibiting cytotoxic activity of lymphocytic cells, inhibiting production of inflammatory cytokines and inflammatory responses associated with those cytokines, inhibiting the activity of heme-containing enzymes and delaying the onset of an autoimmune disease. By combining the subject compositions with mixtures of cells comprising lymphocytic cells and cells which would otherwise activate the lymphocytic cells, lysis of the target cells can be substantially inhibited. The oligopeptides may be joined to a variety of other groups or compounds for varying the activity of the subject composition. The subject compositions may be administered by any convenient means to inhibit lymphocytic attack on tissue, particularly involved with xenogeneic or allogeneic transplants or to inhibit the production of inflammatory cytokines and inflammatory responses associated therewith. The subject compositions may also be used in the inhibition of the activity of heme-containing enzymes.
US7727964 Peptides substituted with a functional group that reacts with an active site residue of the targeted protease, e.g., Cyclohexylglycine BoroAla, and compounds that can hydrolyzed to produce them; improved specificity for regulating glucose metabolism The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
US7598386 Sulphones which modulate the action of gamma-secretase Novel sulphones of Formula I are disclosed: wherein A completes a 4-7 membered ring optionally comprising up to two heteroatoms. The compounds modulate the action of γ-secretase and are therefore useful in the treatment or prevention of Alzheimer's disease.
EP1068202B1 1-(3-heteroarylpropyl- or -prop-2-enyl)-4-benzylpiperidines used as nmda receptor antagonists The invention relates to piperidine derivatives of formula (I) and to the physiologically acceptable salts thereof, whereby X, Y, Z, R?1, R2, R3 and R4¿ have the meanings cited in Claim 1. The inventive piperidine derivatives and the salts thereof can be used as excitatory amino-acid antagonists to combat neurodegenerative disorders including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease or Huntingdon's disease, cerebral ischaemia, infarcts or physchoses.
WO2010103094A1 PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS The invention relates to compounds of Formula (I) wherein X, R1, R2, T, m, n, o have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
EP2146740A1 Methods of controlling tumorigenesis and diagnosing the risk thereof The present invention relates to methods of controlling tumorigenesis, including preventing, inhibiting, arresting or reversing tumorigenesis. The present invention also provides methods of treatment, prevention and diagnosis of neoblastoma, including cancer, such as metastatic cancer. In one method one or more cells having a predisposition to turn tumorigenic are identifyied. In the one or more cells an altered amount, an altered subcellular localisation or an altered activity of a Rab binding protein is detected. In a method of diagnosing the risk of developing a neoplasmt at least one of the expression level, the activity level and the subcellular localisation of a Rab binding protein is determined. In an in-vitro method of identifying a compound capable of forming a complex with a Rab binding protein the components that form the respective complex are contacted with each other. In a method of determining whether a neoplasm is sensitive to an alteration of intracellular calcium levels, at least one of the expression and the activity of a Rab binding protein is determined. An altered expression or an altered activity of the Rab binding protein is an indication that the neoplasm is sensitive to an alteration of intracellular calcium levels.
US20100125086 Use of isoqc inhibitors The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinising polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.
US20100076062 Use of a Truncated eIF-5A1 Polynucleotide to Induce Apoptosis in Cancer Cells The present invention relates to the combinatorial use of an siRNA targeted against an endogenous gene to knock out or knock down expression of the endogenous gene in a host and a delivery of a polynucleotide encoding the gene in a delivery vehicle/expression vector to the host to provide expression in the host of the protein encoded by the polynucleotide. The present invention also relates to a truncated form of eIF-5A1 that is useful for inducing apoptosis and killing of cells, especially cancer cells in a mammal.
US8389003 Ingestible implement for weight control An orally administrable implement for expanding in a stomach of an animal, including a mammal, to fill a space in the stomach, is provided for weight control. The implement includes: a fluid-permeable expandable container having a first dimension and a second dimension; and a plurality of clusters comprising a swellable material contained within the container and capable of swelling when contacted with a fluid; whereby when the implement is ingested, the fluid in the stomach enters the container causing the clusters therein to swell and the container to expand from the first dimension to the second dimension.
CN1582921A Use and medicinal composition of eremophilane lactone for inhibiting hepatitis B virus An application of the particular lactone extracted from senecie in preparing the medicine for suppressing hepatitis B virus and treating hepatitis B is disclosed. Said composite medicine is also disclosed.
WO2008149053A1 Bicycl0 [2. 2. 1] he pt- 2-ylamine derivates and their use A named compound of formula (I): having M3 receptor antagonist activity; a composition comprising such a compound; the use of such a compound in therapy (such as asthma or COPD); and a method of treating a patient with such a compound.
CN101780053A Cefmetazole sodium suspension injection powder and novel application thereof The invention provides cefmetazole sodium suspension injection powder and a preparation method thereof. The cefmetazole sodium suspension injection powder comprises the following components by weight part: 10 parts of cefmetazole sodium, 5 to 30 parts of biodegradable polymer receivable on pharmacy, 1 to 20 parts of emulsifier, 6 to 12 parts of emulsion assistant and 2 to 30 parts of skeleton agent. The cefmetazole sodium suspension injection powder has the application for treating body extensive Psoriasis Pustulosa.
WO2008157271A1 Deuterium-enriched escitalopram The present application describes deuterium-enriched escitalopram, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20090076055 Deuterium-enriched vinflunine The present application describes deuterium-enriched vinflunine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2007012650A1 Isotopically substituted proton pump inhibitors The invention relates to benzimidazoles of Formula (1) and to pharmaceutical compositions comprising these compounds, further to intermediates of Formula (2 and 3).
CA2150785C Conjugates of methyltrithio antitumor agents and intermediates for their synthesis This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
CN1980679A Glycyrrhizin-containing suppository compositions for rectal infusion A glycyrrhizin-containing suppository composition for rectal infusion which comprises at least one member selected from among glycyrrhizin and pharmaceutically acceptable salts thereof, a nonionic surfactant, an oily base, and water and which exhibits a solid-liquid phase transition point of 10 to 4500Pa at 37 DEG C; and a glycyrrhizin-containing suppository composition for rectal infusion which comprises at least one member selected from among glycyrrhizin and pharmaceutically acceptable salts thereof, an oily base, water, and an alkali.
CN101653580B Medicament for curing stomach illness and preparation thereof The invention provides a medicament for curing stomach illness and a preparation thereof. The medicament consists of myrobalan (roasted), alcite, pterocephalus hookeri hook, trogopterus dung ointment, elecampane, seed of pomegranate, pawpaw, tambac, clove, travertine, safflower, nutmeg, katsumadai seed and tsaoko cardamom nutlet. The preparation method comprises the following steps: pulverizing the myrobalan (roasted), the alcite, the pterocephalus hookeri hook, the elecampane, the seed of pomegranate, the pawpaw, tambac, the clove, the travertine, the safflower, the nutmeg, the katsumadai seed and the tsaoko cardamom nutlet in an ultra micro way; evenly mixing; adding with the trogopterus dung ointment and normal auxiliary materials; and preparing clinically acceptable medicament form according to a normal technology. The medicament composite is clinically proved to have a good effect for curing the stomach illness, a fast effect, a short treatment period and no side effect.
CN103251553A Aqueous solution of silybin glycocides and external skin treatment composition An aqueous solution of silybin glycocides with excellent pigmentation stability combines silybin glycocides with one or two substances from the class group comprising polyoxyalkylene diglyceryl ether, dipropyleneglycol, 1, 2-hexanediol, 1, 2-pentanediol, polyethylene glycol, polyoxyethylene methyl glucoside, and 1, 3-butanediol.
CN101912584A Medicine for treating melancholia and preparation method thereof The invention discloses a medicine for treating melancholia. The medicine is mainly prepared from the following raw medical materials in parts by weight: 1-20 parts of roses, 1-20 parts of seville orange flowers, 1-20 parts of lilies, 1-20 parts of tulips, 1-20 parts of bitter oranges, 1-20 parts of balloon flowers, 1-20 parts of hemlock parsley, 1-20 parts of angelica, 1-20 parts of white peony root, 1-20 parts of selfheal, 1-20 parts of cuttlefish bone, 1-20 parts of raw oysters, 1-20 parts of bupleurum and 1-20 parts of over 95% edible alcohol. The medicine can be taken orally and absorbed by the spleen and the stomach or externally used and absorbed by the skin, or can be absorbed in a combined mode of internal taking and external use. The medicine of the invention has reasonable formula, compact and simple matching and accurate cure effect and treats both principal and secondary aspects of the disease. The invention also provides a preparation method of the medicine.
US7078400 20-hydroxyeicosatetraenoic acid (HETE); useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases. In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.
US20110123468 Use of benzotropolone derivatives as uv absorbers and antioxidants and their use in sunscreens and/or cosmetic compositions Described is the use of benzotropolone and their derivatives, especially the compounds of formula (1); wherein R2, R3, R4, R5 and R6 independently of one another are hydrogen; OH; C1-C30alkyl, C2-C30al-kenyl, C1-C30alkoxy, C3-C12cycloalkyl or C1C30hydroxyalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C6-C20aryl, which may be substituted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G, C2-C18alkenyl, C2-C18alkynyl, C7-C25aralkyl, CN, or —CO—R17; C1-C30mono- or dialkylamino; COR9; COOR9; CONR9R10; CN; SO2R9; OCOOR9; OCOR9; NHCOOR9; NR9COR10; NH2; *—(CO)—NH—(CH2)n1—(PO)—(OR11)2; —(CO)—O—(CH2)n1—(PO)—(OR11)2; sulphate; sulphonate; phosphate; phosphonate; —(CH2)n2—[O—(SO2)]n3—OR11; —O—(CH2)n4(CO)n5—R11; —(O)n6—(CH2)n7—(PO)—(OR9)2; —(O)n6—(CH2)n7—SO2—OR9; halogen; organosilanyl; organo-siloxanyl; or a sugar residue linked directly in an α- or β-mode via the anomeric oxygen to the benzotropolone system or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar-(CH2)n—(X1)1 or 0-benzotropolone system, wherein n=1-10 and X1=—O—; —(CO)—; —O—CO—; —COO—, —NH—; —S—; —SO2—); R1, R7 and R8 independently of one another are hydrogen; C1C12alkyl or C3-C12-cycloalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C6-C20aryl, which may be substituted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G, C2-C18alkenyl, C2-C18alkynyl, C7-C25aralkyl, or COOR9; COR9; CONR9R10; SO3R9; SO2R9; PO3(R9)2; PO2(R9)2; organosilanyl; organosiloxanyl; or a sugar residue linked directly in an α- or β-mode via the anomeric oxygen to the benzotropolone system or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar-(CH2)n—(X2)1 or 0—*, wherein n=1-10 and X2=—C(═O)—; —O—CO—*); R9 and R10 independently from each other are hydrogen; C1C18alkyl or C3-C12-cycloalkyl which may be substituted by one or more E and/or interrupted by one or more D; C6-C20aryl, which may be substituted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G; organosilanyl; organosiloxanyl; or a sugar residue linked directly in an α- or β-mode via the anomeric oxygen or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar-(CH2)n—*, wherein n=1-10); or R9 and R10 together form a five or six membered ring, R11 is hydrogen; or C1-C5alkyl; n1, n2, n4 and n7 independently from each other are a number from 1 to 5; n3, n5 and n6 independently from each other are a 0; or 1; D is —CO—; —COO—; —S—; —SO—; —SO2-; —O—; —NR14—; —S1R19R20—; —POR11—; —CR12═CR13—; or —C≡C—; and E is —OR18; —SR18; —NR14R15; —NR14COR15; —COR17; —COOR16; —CONR14R15; —CN; halogen; Or SO3R18; SO2R18; PO3(R18)2; PO2(R18)2; organosilanyl; organosiloxanyl; or a sugar residue linked directly in an α- or β-mode via the anomeric oxygen or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar-(CH2)n-(X1)1 or 0—*, wherein n=1-10 and X1=—O—; —C(═O)—; —O—CO—; —COO—; —NH—; —S—; —SO2—); G is E; C1-C18alkyl, which is optionally interrupted by D; C1-C18perfluoroalkyl; C1-C18alkoxy, which is optionally substituted by E and/or interrupted by D; wherein R12, R13, R14 and R15 independently of each other are hydrogen; C6-C18aryl which is optionally substituted by OH, C1-C18alkyl or C1-C18alkoxy; C1-C18alkyl, which is optionally interrupted by —O—; or Ri4 and Ri5 together form a five or six membered ring, Ri6 is hydrogen; C6-Ci8aryl which is optionally substituted by OH, C1-C18alkyl or d-C18alkoxy; C1-C18alkyl which is optionally interrupted by —O—; R17 is H; C6-C18aryl which is optionally substituted by OH, C1-C18alkyl or C1-C18alkoxy; or d-C18alkyl which is optionally interrupted by —O—; R18 is hydrogen; C6-C18aryl, which is optionally substituted by OH, C1-C18alkyl or d-C18alkoxy; C1-C18alkyl, which is optionally interrupted by —O—; R19 and R20 independently of each other are hydrogen; C1-C18alkyl; C6-C18aryl which is optionally substituted by C1-C18alkyl; and R21 is C1-C18alkyl; or C6-C18aryl, which is substituted by C1-C18alkyl; * means, that this radical is directed to the benzotropolone moiety; for the protection of human and animal hair and skin against UV radiation.
CN103520711A Formula composition and medicinal preparation with effects of increasing bone density and treating bone joint pain, preparation method of medicinal preparation and application of formula composition The invention relates to the field of medicines and health care food, and particularly relates to a formula composition and a medicinal preparation with effects of increasing bone density and treating bone joint pain, a preparation method of the medicinal preparation and an application of the formula composition. The formula composition comprises N-sulfo-glucosamine potassium salt, calcium carbonate, collagen, fructus psoraleae extractive, and casein phosphopeptides. The formula composition can be prepared into various dosage forms to be used as medicines or health care food. The formula composition and the medicinal preparation thereof can effectively increase bone cell proliferation and the bone density, prevent various kinds of discomfort caused by bone loss and relieve bone joint pain, and have no toxic or side effects.
US20130053384 Certain Chemical Entities, Compositions, and Methods Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of using these chemical entities, e.g., for treatment of cancer are described.
CN102151266A Oral liquid for treating white scour of chicken and preparation method thereof The invention discloses an oral liquid for treating white scour of chicken and a preparation method thereof, aiming at providing an oral liquid which can be used for treating white scour infection of chicken with treatment of both principal and secondary aspects of disease and is convenient for medicate and a preparation method thereof which has a simple process and is easy to realize. The composition of each 100L of oral liquid is as follow: 1-7kg of enrofloxacin, 5-15kg of sulfamonomethoxine, 1-3kg of TMP (Trimethoprim), 0.1-0.5kg of atropine sulfate, 30L of dimethylformamide, 20L of 95% ethanol, 1-2kg of sodium hydroxide and the balance of water. In the oral liquid disclosed by the invention, all ingredients are combined and reasonably proportioned to play a multiaspect role on the white scour of chicken with treatment of both principal and secondary aspects of disease; in addition, the oral liquid is a compound preparation and can reach the effect of a plurality of medicines through once administration; and the oral liquid is convenient to use and can ease clinical symptoms when chicken are sicken. The oral liquid disclosed by the invention can intersoluble with water according to any proportion and can be medicated in mass group.
EP2609098A1 Triazolopyrazine derivatives Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment rheumatoid arthritis.
CN102895359A Health capsule The present invention discloses a health capsule, which comprises the raw materials, by mass, 5-8 parts of indigowoad root, 6-8 parts of weeping forsythia fruit, 1-3 parts of borneol, 2-4 parts of plant soot, 2-5 parts of balloonflower root, 3-6 parts of licorice root, 2-4 parts of nacreous layer powder, 3-5 parts of common gardenia fruit, 1-4 parts of cablin potchouli herb, and 4-8 parts of catechu. The capsule has effects of heat clearing, detoxification, phlegm expelling, cough relieving, summer heat dispelling, exterior syndrome relieving, liver protection, cholaneresis, blood pressure lowering and the like, and is a health capsule suitable for all ages.
DE102005012681A1 New 1,5-dihydro-pyrrol-2-one compounds are HDM2 inhibitors, useful for treating e.g. stroke, heart infarct, ischemia, multiple sclerosis, Alzheimer's disease, degenerative disease, viral infection and cancer 1,5-Dihydro-pyrrol-2-one compounds (I) and their salts and esters are new. 1,5-Dihydro-pyrrol-2-one compounds of formula (I) and their salts and esters are new. R1>, R2>cycloalkyl, heteroalkyl, (hetero)aryl or (hetero) arylalkyl; and R3>(hetero)alkyl, cycloalkyl, (hetero)aryl or (hetero)arylalkyl. Independent claims are also included for compounds (I) in combination with one or more anti-tumor agents or one or more antiviral agents. [Image] - ACTIVITY : Cerebroprotective; Vasotropic; Cardiant; Neuroprotective; Nootropic; Virucide; Cytostatic. - MECHANISM OF ACTION : HDM2 inhibitor. Tests details are described but no results are given.
US20120064123 Composition for a topical ophthalmic clear colloidal liquid which undergoes a liquid-gel phase transition in the eye The present invention is directed to a topical ophthalmic composition for a liquid comprised of clear colloidal polar nanolipids delivered in submicron sized particles (Nanopids™), aqueous colloidal lubricants, aqueous polymers, emulsifies, and a unique stabilizing buffer system, which undergoes a liquid-gel phase transition in the eye. Said composition is designed to deliver advanced eye lubricants, protect the three (3) layers of corneal film from dryness, and provide a unique system of Dry Eye treatment that addresses and treats all three layers of corneal tear film. Said composition is further designed to provide a superior delivery system of various Active Pharmaceutical Ingredients (APIs), and/or anti-infective/antibiotic/anti-fungal agents, accepted as safe and efficacious for ophthalmic use.
CN101773508B Stable Trifusal pharmaceutical composition The invention discloses a stable trifusal pharmaceutical composition, which is characterized by comprising trifusal, a surface active agent and other receivable carriers on the aspect of the pharmacy. 1000 grains of stable traifusal pharmaceutical composition comprise the following components: 100 to 600 g trifusal, 50 to 200 g lactose, 1 to 12g lauryl sodium sulfate, 1 to 10g magnesium stearate and 1 percent citric acid and 10 percent starch slurry with appropriate quantity. The invention also relates to a preparation method of trifusal capsule. The trifusal tablet which is prepared by the formula and the preparation method has good fluidity, good dissolution, small charge quantity difference, good stability, high biological utilization degree and good curative effect.
WO2014036865A1 Method for preparing fingolimod mucate and crystal thereof and application of fingolimod mucate and crystal thereof The present invention relates to fingolimod mucate, a crystal form A thereof and a preparation method for the fingolimod mucate and the crystal form A thereof. The crystal form A has characteristic peaks in an X-ray powder diffraction pattern obtained by the diffraction of Cu Kα rays when 2θ is about 6.1, 9.1, 12.2, 14.9, 15.7, 17.8, 18.5, 19.6, 20.6, 21.4, 21.8, 22.5 and 24.5 degrees. The present invention also relates to the application of the crystal form A to the preparation of a medicament which is taken as a sphingosine-1-phosphate (S1P) receptor modulator, in particular to the application of the crystal form A to the preparation of a medicament which is taken as an immunomodulator. In addition, the present invention also provides a pharmaceutical composition, which comprises the fingolimod mucate or the crystal form A and a pharmaceutically acceptable carrier.
CN103230408A Method for preparing phloretin The invention provides a method for preparing phloretin. The method comprises the following steps of: heating, hydrolyzing and purifying to obtain the phloretin under the action of dilute acid by using naringin dihydrochalcone. The naringin dihydrochalcone is prepared by the following method: performing catalytic hydrogenation on naringin under the medium pressure, normal temperature or heating action by using hydrogen in the presence of alkali liquor and rare metal catalyst, and collecting the naringin dihydrochalcone from the reaction system. The method is easy to operate, low in cost and high in product quality, and large-scale application of phloretin on the medicine, food and cosmetics can be well met.
US20100035970 Methylation Markers for Diagnosis and Treatment of Cancers Two hundred ten markers are provided which are epigenetically silenced in one or more cancer types. The markers can be used diagnostically, prognostically, therapeutically, and for selecting treatments that are well tailored for an individual patient. Restoration of expression of silenced genes can be useful therapeutically, for example, if the silenced gene is a tumor-suppressor gene. Restoration can be accomplished by supplying non-methylated copies of the silenced genes or polynucleotides encoding their encoded products. Alternatively, restoration can be accomplished using chemical demethylating agents or methylation inhibitors. Kits for testing for epigenetic silencing can be used in the context of diagnostics, prognostics, or for selecting “personalized medicine” treatments.
CN102836161A Medicament compound preparation formed by mixing olmesartan medoxomil with benzene sulfonic acid amlodipine and hydrochlorothiazide The invention relates to a medicament compound preparation formed by mixing olmesartan medoxomil with benzene sulfonic acid amlodipine and hydrochlorothiazide. Both the olmesartan medoxomil and amlodipine are unstable compounds, and are difficultly prepared into mixed medicaments with stable active ingredients. According to the invention, the adjuvant of the olmesartan medoxomil and amlodipine compound preparation is regulated, so that the amounts of degradation products and impurities of the olmesartan medoxomil are effectively reduced. The invention provides a method for preparing the fixed-dose compound preparation which takes the olmesartan medoxomil, the amlodipine and hydrochlorothiazide as the active ingredients.
EP2155707A1 Metabolites of (thio)carbamoyl-cyclohexane derivatives The present invention relates to metabolites of(thio)-carbamoyl cyclohexane derivatives, particularly, metabolites of trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]- ethyl}-N,N-dimemylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing the same and to their use in the treatment and/or prevention of a conditions which requires modulation of dopamine receptors.
CN103565756A Preparation method of miriplatin freeze-drying preparation The invention relates to a preparation method of a miriplatin freeze-drying preparation. The freeze-drying preparation consists of miriplatin as an active ingredient or pharmaceutically acceptable salt thereof, a solvent compound, an enantiomer or raceme, and prodrug or analogue. The freeze-drying preparation is characterized in that the active ingredient is dissolved through a mixing solvent of tert butyl alcohol and methanol, and the solution is freeze-dried, thus obtaining the freeze-drying preparation for sterile injection. The miriplatin freeze-drying preparation prepared by the invention is round and normal in formed spherical particle and uniform in size, and can be easily oil-suspended in iodinated oil; a formed suspension has possibility of getting layered, and the viscosity can not increase along with time.
CA2576640C Bimetal complexes and methods of making them Bimetal complexes useful in the treatment of skin conditions are described. The bimetal complexes are prepared by reacting a polyfunctional acid, amine or amino acid with two or more coordination elements chosen from the elements listed in Groups IIIAto VIIIA, Groups IB to IIIB, of periods 4 and 5 and aluminum in Group IIIB, period 3 of The Periodic Table of the Elements.
CN101467996B Use of deuteroporphyrin derivates The invention belongs to the technical field of medicament and specifically relates to use of a deuteroporphyrin derivative. The invention provides use of deuteroporphyrin derivative in preparing medicament for treating squamous carcinoma or adenocarcinoma. The treatment with the deuteroporphyrin derivative or composition and medicament thereof to squamous carcinoma or adenocarcinoma has obvious growth-inhibiting effect and good dose effect relationship. A group with high dosage has strong and stable effect and stronger inhibiting effect than the positive control medicament, hemoporphyrin. The deuteroporphyrin derivative has no growth-inhibiting effect on tumour cells under a condition of non-laser radiation, no damaging effect on normal histiocytes with light or without light and little side effect.
US20050259281 Method, apparatus and computer program for transforming digital colour images A first digital colour image with pixels having colour values is transformed to a second digital colour image with pixels having transformed colour values, the colour values being defined in a selected colour space. Pixel clusters are formed for the first digital colour image whereby pixels of a pre-defined category are grouped into a particular cluster in the selected colour space. The colour values of the pixels in a particular cluster are transformed such that transformed colour values belong to a pre-defined area associated to the particular cluster in the selected colour space, the pre-defined area consisting of memory colours of the same pre-defined category. The second digital colour image can be rendered on a display screen or on a print medium.
US20130004436 Compositions and Methods of Treating and Preventing Lung Cancer and Lymphangioleiomyomatosis Compositions and methods for treating and preventing cancer, particularly lung cancer, lymphangioleiomyomatosis and asthma are provided.
WO2008101139A1 Sustained-release tablet formulations of piperazine-piperidine antagonists and agonists of the 5-ht1a receptor having enhanced intestinal dissolution The present invention relates to sustained-release tablet formulations of piperazine- piperidine compounds, which can be useful in treating central nervous system disorders; to processes for their preparation; and to methods of using them.
CN101401798A Proanthocyanidin effervescent tablet and preparation method thereof The invention relates to a proanthocyanidin effervescent tablet and a method for preparing the same. The effervescent tablet consists of the following components in the following weight percentage: 2 to 15 percent of proanthocyanidin, 1 to 10 percent of vitamin C, 10 to 40 percent of beta-cyclodextrin, 20 to 50 percent of citric acid, 30 to 35 percent of sodium bicarbonate, 0.5 to 1 percent of protein sugar, 0.1 to 2 percent of flavoring essence, and 0.05 to 0.1 percent of magnesium stearate. The proanthocyanidin effervescent tablet has the advantages that the proanthocyanidin effervescent tablet can be conveniently carried around, used and absorbed as the common effervescent tablets, and simultaneously has characteristics of high concentration of functional substances and strong functionality, as well as bright color of the proanthocyanidin; the proanthocyanidin effervescent tablet has the greatest advantage that the stability of the proanthocyanidin is greatly improved after the proanthocyanidin is embedded by the beta-cyclodextrin; the vitamin C is added in the effervescent tablet to further prevent the proanthocyanidin from being oxidized and act synergistic effect on the antioxidant activity of the proanthocyanidin so as to improve the functionality thereof; furthermore, the proanthocyanidin effervescent tablet has simple formulation, easy preparation, and low cost.
US20110190378 Mir 204, mir 211, their anti-mirs, and therapeutic uses of same Embodiments of the invention provide methods of preventing or treating detrimental epithelial cell proliferation, loss of epithelial cell differentiation, age-related macular degeneration and/or proliferative vitreal retinopathy in an individual comprising administering to an individual in need thereof an effective amount of miR 204, an effective amount of miR 211, or an effective amount of a mixture of miR 204 and miR 211. A further embodiment of the invention provides a method of facilitating the transport of a substance across an epithelium in an individual comprising administrating to an individual an effective amount of anti-miR 204, an effective amount of anti-miR 211, or an effective amount of a mixture of anti-miR 204 and anti-miR 211. Additional embodiments of the invention include pharmaceutical compositions of miR 204 and/or miR 211 and pharmaceutical compositions of anti-miR 204 and/or anti-miR 211.
CA2326348C Liposomal bupivacaine compositions and methods of preparation Liposomal local anesthetic compositions and methods of their preparation and use are described. The compositions, typically for delivery of bupivacaine, are formulations of the drug in DRV (dehydration-rehydration vesicle) liposomes.
CN1723964A Medicine for treating cough and chronic bronchitis A medicine in the form of soft-capsule, dispersing tablet, dripping pill, disintegrating tablet, or effervescent table for treating cough and chronic bronchitis is prepared from the extract of small-leaf banyan and chlorphenamine maleate.
CN101683425A Pharmaceutical composition for treating dorking abdominal dropsy caused by high natrium The invention relates to a pharmaceutical composition for treating dorking abdominal dropsy caused by high natrium, which is prepared by uniformly mixing the following components by weight: 50-400 mgof digitalis leaf ultrafine powder, 10-100 mg of triamterene and 50,000 mg of glucose. In the invention, the digitalis leaves contain digitoxin, thereby strengthening the myocardial contraction force,increasing the cardiac output and also slowing the heart rate and reducing the myocardial oxygen consumption so that heart-failure heart functions are improved; the digitalis leaf ultrafine powder isbeneficial to absorbing, thereby reducing the dosage and the side effects of medicaments and enhancing the treatment effect; the triamterene increases the discharge amount of natrium and chlorine soas to be diuretic, thereby being more suitable for heart-failure dorkings; in addition, the glucose improves the requirement of important organs of organisms for sugar in a high natrium state, therebybeing benefit to the detoxifying function of liver and kidney. The pharmaceutical composition is simple, has reasonable preparation and plays a good role in treating the dorking abdominal dropsy caused by the high natrium contained in the feeds or drinking water after being added to dorking feeds per kilogram.
US20110091510 Nanorod materials and methods of making and using same The subject invention concerns nanorods, compositions and substrates comprising nanorods, and methods of making and using nanorods and nanorod compositions and substrates. In one embodiment, the nanorod is composed of Zinc oxide (ZnO). In a further embodiment, a nanorod of the invention further comprises SiO2 or TiO2. In a specific embodiment, a nanorod of the invention is composed of ZnO coated with SiO2. Nanorods of the present invention are useful as an adhesion-resistant biomaterial capable of reducing viability in anchorage-dependent cells.
CN102743331A Disinfection preparation containing levorotatory folinic acid sodium The present invention relates to a disinfection preparation containing levorotatory folinic acid sodium and a preparation method thereof. The levorotatory folinic acid sodium is a pharmaceutical composition, which is prepared from a main component of levorotatory folinic acid sodium and pharmaceutically acceptable excipients. The disinfection preparation has advantage that an injection disinfection preparation with high level of sterility assurance is prepared by addition of pharmaceutically acceptable stabilizer and inert gas protection and through terminal disinfection process.
EP2068902A2 Tea-derived compostiions and methods of using same for cardiovascular health Disclosed herein are compositions comprising tea derived components which are useful in decreasing elevated blood pressures, lowering LDL and/or lowering inflammatory markers of cardiovascular disease. Specifically exemplified herein are compositions comprising predetermined amounts of L-theanine and EGCG, and methods of using same to improve cardiovascular health.
WO2012139425A1 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoismers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and uses, including Alzheimer's disease, are also disclosed.
US20080214664 Anesthetic spray composition An anesthetic spray composition suitable for application to the back of the throat comprising a topical anesthetic and a mucoadhesive polymer.
CN102872039A Application of Gypensapogenin B in medicaments for promoting insulin secretion The invention belongs to the pharmaceutical filed, and discloses an application of Gypensapogenin B in preparing medicaments against insulin secretion. The application of Gypensapogenin B in preparing medicaments for promoting insulin secretion, involved in the invention, is disclosed for the first time. As the skeleton type is brand new, and the activity of Gypensapogenin B on promoting insulin secretion is unexpectedly strong, the possibility that any enlightenments are given by other compounds does not exist. Gypensapogenin B has prominent substantive features and has notable progress when being used for preventing and treating type 2 diabetes.
CA2703767A1 Novel 4-(tetrazol-5-yl)-quinazoline derivatives as anti cancer agents The invention relates to substituted 4-(tetrazol-5-yl)-quinazolute derivatives of the formula-1, or phannaceutically-acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted 4-(tetrazol-5-yl)-quinazoline derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medica-ments for the production of an anti-proliferative effect in a warm-blooded animal such as man.
EP1605926B1 Use of pinitol for treatment of liver diseases in mammals Disclosed in this invention is a use of pinitol or chiroinositol for protecting the liver.
WO2008139009A1 Pyridothieneotriazines as antiangiogenic compounds Pyridothienotriazines as antiangiogenic compounds. The present invention concerns derivatives of pyridothienotriazines with antiangiogenic activity and use thereof in the preparation of pharmaceutical compositions or medicines for the treatment of diseases involving the angiogenesis process, such as cancer, obesity, diabetic retinopathias, haemangomas, arthritis, psoriasis and atherosclerosis.
WO2014066304A1 Compositions and methods for treating or preventing diseases or disorders associated with misregulated eif4e Disclosed herein are compounds, compositions, formulations, kits and methods of treatment useful for treating or preventing one or more hyperproliferative disorders, e.g., cancer or a neurological disease or disorder.
CN102311475A New compound separated from Mythic Fungus, preparation method thereof and medicinal purpose thereof The invention relates to a new compound separated from Mythic Fungus, a preparation method thereof and a medicinal purpose thereof. The invention discloses a compound with the chemical structural formula shown in the specification. The preparation method of the compound comprises the following steps: 1, extracting Mythic Fungus with alcohol or an alcoholic solution once or more than twice, filtering, collecting a filtrate, carrying out reduced pressure concentration, and drying to obtain an alcohol extract; 2, adding water to the alcohol extract, extracting with petroleum ether for degreasing, extracting with ethyl acetate, extracting an obtained ethyl acetate extract with an aqueous solution of NaHCO3, taking an ethyl acetate phase, and evaporating to dryness to obtain a crude product; and 3, carrying out chromatogram separating separation and purification on the obtained crude product to obtain the compound. The compound of the present invention can be treated as a medicine for treating tumors.
US20080085910 For inflammatory bowel disease; oral administration, bioavailability, pharmacokinetics; 2-(2,6-Dichlorobenzamido)-5-[4-(ethyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid methyl ester for example A glycine derivative which is, e.g., the following compound (Chemical formula (1)). It is highly effective in the treatment and prevention of inflammatory bowel diseases. Compared to conventional compounds, the compound is excellent in absorbability in oral administration and in vivo stability. The compound can be orally administered and can retain an excellent therapeutic or preventive effect over a longer period.
WO2008039937A3 Blocking of gene expression in eukaryotic cells The present invention provides methods for designing a sequence for efficient short interference RNA molecules. In particular, the present invention defines a universal target for siRNA derived from a poly A sequence, optionally in conjunction with unique sequences for gene silencing and inhibition of viral replication in a eukaryotic host cell. The present invention further provides methods for the treatment and prevention of diseases and disorders by silencing a gene of a virus, an oncogene, genes encoding transcription factors and many other diseases related genes. The present invention describes antisense nucleic acids compositions comprising sequences complementary to a target nucleic acid. The antisense sequences are designed to hybridize to complementary nucleic acid target regions in a target RNA, and inhibit translation, processing, transport, or binding by proteins or riboproteins. Target regions include, and are limited to a poly-A tail, and exclude, AUG, 5' non-translated sequences, translation initiation factor binding sites, ribosome subunit binding sites, Shine Dalgarno sequence, 3' nontranslated sequences, poly- addition site, 3' cleavage site, coding region, intron, intron branch site, intron/exon junction, and splice sequence.
CN102532156A Swerilactones H-K, 1-4 and medicinal composition and application thereof The invention discloses a compound shown as a structural formula (I), i.e., swerilactones H-K, 1-4, a medicinal composition consisting of an effective amount of the compound 1-4 and a medicinal carrier or an excipient, preparation methods of a medicinal compound, i.e., swerilactones H-K (1-4) and the medicinal composition thereof, an application of the swerilactones H-K, 1-4 to treatment of human diseases, and particularly an application of the swerilactones H-K, 1-4 to preparation of a medicament for resisting virus B hepatitis and a medicament for treating virus B hepatitis.
US7135472 3-Heterocyclic benzylamide derivatives as potassium channel openers The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said novel 3-heterocyclic benzylamides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.
CN1559400A Method for preparing scutellarein liquid A scutellarein liquid for regulating immunity, protecting liver and gallbladder, and treating soft tissue injury, infection and tumor is prepared through proportionally mixing scutellarein, antioxidizing agent and the water for injection, regulating pH=6.5-8.5, adding activated carbon, keeping the temp at 60-80 deg.C for 1 hr, cooling for one week and filter.
CA2806740A1 Use of rasagiline for the treatment of olfactory dysfunction Disclosed are methods of treating olfactory dysfunction by periodically administering a therapeutically effective amount of rasagiline or a pharmaceutically acceptable salt of rasagiline to a subject.
US7022678 Pregabalin lactose conjugates In accordance with the present invention, there is provided pregabalin lactose conjugate compounds. Also provided as part of the present invention is a novel method of central nervous system disorders or diseases including seizure disorders, pain, depression, anxiety, sleep disorders, consumptive disorders, psychosis, tardive dyskinesia, Huntington's disease, or Parkinson's disease in a subject by administering to the subject a pharmaceutically effective amount of a pregabalin lactose conjugate.
US20060287361 Diarylmethylidene piperidine derivatives, preparations thereof and uses thereof as opoid receptors ligands Compounds of general formula: (I) wherein R1, R2, R3 and A are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the treatment of pain and anxiety.
US20090281129 Cdki pathway inhibitors and uses thereof The invention relates to the inhibition of the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.
CN101492448B 7'-aza indirubin compounds for antineoplastic medicament The invention relates to a 7'-aza-indirubin compound applied to anti-tumor drugs, belonging to the pharmaceutical chemistry technical field. On the basis of compound indirubin mother nucleus structure with anti-tumor function, nitrogen atoms are introduced into bit 7' to synthesize a serial of totally novel 7'-aza-indirubin compounds with anti-tumor activity and salts thereof which are acceptable in pharmacy. The new compounds and the salts thereof with the structural formula as is shown above can be applied to drugs for treating tumors.
US20120202870 Treatment of inflammatory diseases using mir-124 Methods of treating, reducing the risk of developing, or delaying the onset of an inflammatory disease are disclosed. The methods involved providing a subject with or at risk of developing an inflammatory disease and administering to the subject an effective amount of a first therapeutic composition comprising miR-124. Further provided are methods of diagnosing a subject with or at risk of developing an inflammatory disease.
CN1569002A Dripping pills of flurazepam hydrochloride and its preparation method The invention relates to a Fluoxetine Hydrochloride drop pill prepared by utilizing ultramicro disintegration and drop pill manufacturing process, which has the advantages of improving collapse and dissolving speed, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use. It has good compliance, thus is especially suitable for children, the elderly, bedridden patients and dysphagia patients.
EP1966203A2 Oxazoloisoquinoline derivatives as thrombin receptor antagonists Heterocyclic-substituted bi or tricyclics of the formula (I) or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein ------ represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein An, Mn, Un, Gn, Jn, Kn, R9, R10, R11, R32, R33, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
US20080193463 Combating the pathogenic effects of Mycoplasma infection in an animal by administering an effective amount of isolated and purified mycoplasmal L-alpha-glycerophosphate oxidase or an immunogenic fragment thereof, and a pharmaceutically acceptable carrier The present invention relates i.a. to vaccines for combating Mycoplasma infection, to mycoplasmal L-α-glycerophosphate oxidase for use in such vaccines, to the use of mycoplasmal L-α-glycerophosphate oxidase for the manufacturing of such vaccines, to methods for the preparation of such vaccines and to diagnostic tests for the discrimination of animals vaccinated with said vaccines and animals vaccinated with whole cell vaccines or animals suffering from field infection.
CA2222650C Tnf-.alpha. converting enzyme A metalloprotease that converts TNF-.alpha. from the 26kD cell form to the cell form to the 17 kD form has been isolated and purified and the cDNA sequence known. In particular, the protease has a molecular weight of approximately 80 kD. The isolated and purified protease is useful for designing an inhibitor thereof, and may find use as a therapeutic agent. Assays for detecting the protease-inhibiting activity of a molecule are also an aspect of the invention.
US20110045074 Matrix type sustained-release preparation containing basic drug or salt thereof and, method for manufacturing the same A matrix type sustained-release preparation and a manufacturing method therefor are provided wherein dissolution with low pH dependence of a basic drug or a salt thereof at the early stage of dissolution can be ensured in a dissolution test, and wherein as the dissolution test proceeds, a ratio of a dissolution rate of the basic drug or the salt thereof in an acidic test solution to a dissolution rate of the basic drug or the salt thereof in a neutral test solution (dissolution rate in the acidic test solution/dissolution rate in the neutral test solution) decreases with dissolution time at the late stage of dissolution, as compared to the early stage of dissolution. According to the present invention, the matrix type sustained-release preparation contains a basic drug or a salt thereof and at least one enteric polymer, in which solubility of the basic drug or the salt thereof in a 0.1 N hydrochloric acid solution and a neutral aqueous solution, pH 6.0 is higher than in a basic aqueous solution, pH 8.0.
EP1619244A1 Method for inducing neural differentiation The present invention provides a method for inducing neural differentiation comprising treating a bone marrow stem cell with a neurotrophic factor and/or dibutyryl cAMP (dbcAMP), wherein the neurotrophic factor comprises glial cell line-derived neurotrophic factor (GDNF) or pituitary adenylate cyclase-activating polypeptide (PACAP).
CN101591375A Compound with analgesic activity, preparation method and application thereof The invention discloses a general formula I compound with analgesic activity and also discloses an intermediate compound of the general formula I compound, preparation method and application thereof in medicine, belonging to the biomedicine field. Pharmacological trials sow that the general formula I compound of the invention has excellent analgesic activity and is the potential clinical analgesic agent.
WO2006129876A1 Body odor improving agent for ingestion into body, beverage/food using the same, and method for improvement body odor Disclosed are: a body odor improving agent for application through the ingestion into the body which comprises a body odor improving substance and can improve the body odor by releasing the substance through the body surface, wherein the body odor improving substance is at least one of a polar compound and a terpene; a beverage/food comprising the body odor improving agent; and a method for improving the body odor comprising ingesting at least one of a polar substance and a terpene into the body and releasing the substance through the body surface. Thus, it becomes possible to provide a body odor improving agent for ingestion into the body which ensures the improvement in body odor in a simple manner merely by ingesting the agent into the body to release a body odor improving substance from the body surface, which is safe, and which exerts little influence on the flavor or texture of a beverage/food when applied to the beverage/food; and a beverage/food and a body odor improving method using the body odor improving agent.
US7294638 Treatment of ADHD The use of 3-[1-[2-(1-acetyl-2,3-dihydro-1H-indol-3-yl)ethyl]-1,2,3,6-tetrahydropyridin-4-yl]-6-chloro-1H-indole, any of its enantiomers and pharmaceutically acceptable salts thereof for the preparation of a pharmaceutical composition for the treatment of attention deficit hyperactivity disorder.
US7129361 Thienylazolylalkoxyethanamines, their preparation and their application as medicaments The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.
WO2008120720A1 Dentinogenesis promoter and dentinogenic pulp-capping material It is intended to provide a dentinogenesis promoter, which is effectively usable in forming (regenerating) the dentin, and a dentinogenic pulp-capping material. It is also intended to provide a method of producing odontoblasts which are useful in a tooth regenerative therapy and use of the odontoblasts thus obtained. The above-described dentinogenesis promoter and dentinogenic pulp-capping material are each characterized by containing an HMG-CoA reductase inhibitor as the active ingredient. Odontoblasts can be produced by culturing cells, which can be differentiated into pulp cells, in the presence of an HMG-CoA reductase inhibitor.
WO2013058674A1 Bicarbonate haemodialysis solution The invention relates to an acid component for bicarbonate dialysis comprising at least hydrochloric acid, citric acid and succinic acid, as well as to a concentrate for the preparation of bicarbonate haemodialysis solutions and a method for producing said acid component for bicarbonate haemodialysis.
EP1631331A1 A bioabsorbable delivery system This invention relates to bioabsorbable materials and implants used to prevent and treat infection and promote bone growth. More specifically, this invention relates to synthetic bioabsorbable drug delivery materials and implants comprising: (a) a synthetic bioabsorbable polymeric matrix; (b) an antibiotic phase dispersed into said polymeric matrix; and (c) antibacterial, bioabsorbable, bioactive glass, dispersed into said polymeric matrix for the promotion of bone growth.
US20050249700 Blockade of T lymphocyte down-regulation associated with CTLA-4 signaling T cell activation in response to antigen is increased by the administration of binding agents that block CTLA-4 signaling. When CTLA-4 signaling is thus blocked, the T cell response to antigen is released from inhibition. Such an enhanced response is useful for the treatment of tumors, chronic viral infections, and as an adjuvant during immunization.
US20070004743 Intranasal administration of mc4-r agonists A method for delivering a melanocortin-4 receptor agonist to a mammalian subject, includes administering the melanocortin-4 receptor agonist to a tissue inside the nasal cavity or sinuses of the mammalian subject. In some instances, the melanocortin-4 receptor agonist includes a guanidine functional group.
WO2010050456A1 Piperidine compound having di- or tri-arylmethyl structure A melanin-concentrating hormone receptor antagonist which is useful as a pharmaceutical product for central nervous system diseases, cardiovascular diseases and metabolic diseases. Z: a C1-6 alkyl, an aryl or the like W: an H, an OH, an NH2 or the like Ar1: a 6-membered aryl or the like Ar2: a 6-membered heteroaryl or the like R1a-R3a, R1b-R3b: an H, a C1-6 alkyl or the like Y1, Y2: an H or the like; or combined together to form an -O-CH2- or the like ring A: a benzene ring, a pyridine ring or the like
WO2013090991A1 Tgf-beta therapy A method of minimising inflammation in one or more tissues of an individual including selecting and/or providing an individual having one or more inflamed tissues, and in which the one or more inflamed tissues have been treated to deplete substantially all beta-catenin/Smad3 complexes in the tissues; applying TGF-beta1 to said one or more tissues in an amount effective for inducing an anti-inflammatory response in said one or more tissues, thereby minimising inflammation in said one or more tissues of said individual.
US20080020025 Composition for wound care and method of using same This invention encompasses an expeditious method and composition for treating a wide variety of wounds and injuries by promoting the elevation of pH at the site of injury, enhancing the reduction or elimination of pain and scaring from the patho-physiological process of infection proliferation, and promoting enhanced wound care management and wound healing. The invention also provides a method of treating a subject having a condition associated with the presence of free radicals in quantities sufficient to cause undesirable symptoms. The invention encompasses controlling mechanisms of intracellular and extra-cellular ionic physiology through the administration of a composition which includes alkaline salts preferably cesium salts, for pH modulating and for restoring and enhancing the localized cellular ionic physiology. The composition promotes the increase of the electrical current density to certain types of wounds and also functions to treat and/or prevent adhesions resulting from surgeries. The composition simultaneously normalizes the localized ionic environment, thereby normalizing immune responses and reducing acidotic induced pain.
CN102626410A Pharmaceutical composition containing roflumilast The invention relates to a pharmaceutical composition containing roflumilast. The pharmaceutical composition containing roflumilast has good dissolution effects and comprises components of roflumilast, water-soluble excipients and water-soluble polymer adhesives, wherein roflumilast is subjected to micronization so that 90% or more by volume of roflumilast particles have particle sizes of 5 to 50 microns and preferably have particle sizes of 10 to 20 microns. The pharmaceutical composition containing roflumilast has good dissolution effects so that the bioavailability of the pharmaceutical composition containing roflumilast is improved effectively.
EP2404604A1 Salts of potassium ATP channel openers and uses thereof Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
US20090118248 3-Alpha-hydroxy 21-n-heteroaryl-pregnane derivatives for modulation of brain excitability and a process for the production thereof The invention relates to a novel multi step process of making compounds of Formula I: wherein R1 is an alkoxy group and R2 is an optionally substituted, N-attached heteroaryl. The hydrogen at the 5-position can be α or β isomer, preferably α. Preferably the compound of Formula I is 17β isomer. The invention also relates to novel 3α-hydroxy-3β-substituted-17-substituted steroid compounds having GABAA receptor modulating activity, pharmaceutical compositions comprising these compounds, and the use of these compounds in a method of modulating brain excitability.
US7019135 For therapy of viral infection Compounds of the general formula (I) are described wherein R, R′, R″, Q, T, T′, T″, T″′, W, X, and Z are as defined in the specification. Compounds according to the invention preferably display potent anti-viral activity against, for example, cytomegalo virus.
CN1839853A External use medicine for treating acne The invention discloses an externally used medicament for treating acne, wherein the constituents comprise (by weight ratio): 2-3% of chloromycetin ethanol solution 1.5-2.5, 0.14-0.18% of gentamicin salt aqueous solution 0.8-1.2, 0.1% chlorpheniramine salt aqueous solution 0.8-1.2.
CN1806803A Perphenazine orally disintegrating tablet and preparation method thereof The invention discloses a Perphenazine oral disintegrating tablet, which is prepared from 2.0-10.0 wt% of Perphenazine, 20.0-30.0wt% of sodium carboxymethylstarch, 50.0-70.0wt% of crystalline cellulose, 5.0-10.0wt% of miropowdered silica gel, 0.5-2.0wt% of magnesium stearate, and 0.1-0.5 wt% of polysorbate through passing through 100 mesh sieves, mixing homogenously, and carrying out powder direct pelleting method to obtain the composition.
US20060241132 Spiro derivatives and adhesion molecule inhibitors comprising the same as active ingredient Disclosed is the use of an adhesion molecule inhibitor that is effective in the prevention and treatment of inflammatory diseases caused by infiltration of leukocytes such as monocytes, lymphocytes and eosindphils, by inhibiting cell infiltration which mediates adhesion molecules, especially adhesion molecule VLA-4. Since the spiro acid derivatives according to the present invention are excellent in the effect of inhibiting cell adhesion via adhesion molecules, especially adhesion molecule VLA-4, they are useful as therapeutic drugs against various inflammatory diseases. For example, provided are the spiro derivative and the adhesion molecule inhibitor which includes as an active ingredient the spiro derivative as shown by the below formula (18).
US20100249060 Topical formulation of low level clobetasol propionate for treating disorders of the skin and mucous membranes A new topical formulation is provided, with a high chemical stability, of for example a low dose clobetasol propionate, suitable for the topical treatment of skin and mucous membrane conditions associated with disorders including psoriasis, eczema, and other forms of dermatitis and also topical use associated with the mouth, such as lichen planus. The formulation includes an aqueous vehicle of based on propylene glycol as a solvent and moisture-retaining agent, and macrogol-glycerol hydroxystearate as a non-ionic emulsifier, being capable of holding surprisingly low concentrations of clobetasol. The vehicle holds concentrations about 0.005% to about 0.05% by weight of 17-clobetasol propionate, more preferably about 0.02 to 0.025%, even more preferably 0.025% by weight of 17-clobetasol propionate. The formulation has a good chemical stability, resulting in a long durability.
US7105484 GDNF receptorα GDNFRα, GDNFRα extracellular domain (ECD), GDNFRα variants, chimeric GDNFRα (e.g., GDNFRα immunoadhesin), and antibodies which bind thereto (including agonist and neutralizing antibodies) are disclosed. Various uses for these molecules are described, including methods to modulate cell activity and survival by response to GDNFRα-ligands, for example GDNF, by providing GDNFRα to the cell. Also provided are methods for using GDNFRα, GDNF, or agonists thereof, separately or in complex, to treat kidney diseases.
US20100316694 Novel filter composites for drug detoxification A filter and a method of forming a suture structure. The filter includes layered structure(s) interior to the filter. Each layered structure includes a carbon structure comprising carbon and a coating on a surface of the carbon structure. Each layered structure may further include a heparin layer that includes heparin and is on the coating. The coating of the filter includes cellulose, PMMA, PEMA, or PHEMA. The carbon structure may include an activated charcoal layer or carbon nanotube(s). The layered structure is configured to remove a contaminant flowing through the filter. The method of forming the suture structure includes forming a film on a suture that has been previously formed on a mammal. The film includes both a coating on the suture and a heparin layer that includes heparin and is on the coating. The coating of the suture structure includes cellulose, PMMA, PEMA, or PHEMA.
CN101862346B Hypoglycemic application of gingseng acidic polysaccharide The invention discloses hypoglycemic application of gingseng acidic polysaccharide. The hypoglycemic gingseng acidic polysaccharide is prepared by using gingseng as a raw material by the steps of extraction, purification and refining. The gingseng acidic polysaccharide of the invention can be prepared into various gingseng acidic polysaccharide preparations with hypoglycemic effects. The method retains the activities of the gingseng acidic polysaccharide and improves the purity of the hypoglycemic active ingredient of the gingseng polysaccharide.
WO2011159124A3 Novel benzoxazole derivative having inhibitory activity against interleukin-6, preparation method thereof, and pharmaceutical composition containing same The present invention provides a benzoxazole derivative represented by formula 1 which has an inhibitory activity against interleukin-6, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The compound represented by formula 1 according to the present invention has an excellent inhibitory activity against interleukin-6, and thus can be used to prevent and treat diseases caused by the abnormal activity of interleukin-6.
WO2009082347A1 Bis- (sulf onylamino) derivatives for use in therapy The invention provides compounds of formula (I) wherein R1,R3,L1,L2,G1,G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
CN102018780B Skin bacteriostatic agent and preparation method thereof The invention discloses a skin bacteriostatic agent, and simultaneously discloses a preparation method of the skin bacteriostatic agent. Per L of the skin bacteriostatic agent is prepared from the following raw materials: 15-20g of moxa leaves, 1-3g of cordyceps sinensis, 3-6g of red flower, 3-6g of radix clematidis, 3-6g of broom cypress fruit, 5-10g of common cnidium fruit, 2-6g of radix sophorae flavescentis, 3-8g of angelica sinensis, 100ml of propylene glycol, 6-10g of 1-n-Dodecylazacycloneptan-2-ketone, 60g of salicylic acid, 30-50g of dyclonine, 1-5g of phenol, and the balance of 75% ethanol water solution. The skin bacteriostatic agent provided by the invention has obvious curative effect, can be used for treating various skin diseases, and has the advantages of wide use range, short treatment course, instant effect, and no toxic and side effect; and the disease can not relapse after being treated.
US20080070856 Medicament to treat a fibrotic disease The invention relates to a drug for treating a fibrotic disease, said drug containing a double straded ribonucleic acid (dsRNA) suitable for inhibiting, through RNA interference, the expression of a gene involved in the formation of extracellular matrix.
US20120295869 Sterile Hyaluronic Acid Solutions Sterilized aqueous solution comprising 0.04% to 0.8% by weight hyaluronic acid with a weight average molecular weight from 0.6 MDa to 3.6 MDa, and one or more buffer components selected from the group consisting of boric acid, sodium borate and sodium dihydrogen phosphate. The aqueous solution also has an ionic strength equivalent to an aqueous concentration of sodium chloride from 4% to 18% by weight of sodium chloride and a pH from 6.4 to 7.2. The solution is also filtered through a filter medium that has an average pore size of 0.25 μm or less to provide a sterilized high salt, hyaluronic acid solution.
CN1611225A Swallow foot beauty and free radical cleaning function The present invention finds special application of Yanzi cactus extract (CAE) with the functions of beautifying face and removing human and animal internal active oxygen (free radical). In order to prevent free radical from persecuting and injuring human body and animal body said invention provides a CAE preparation for excellently promoting growth of hydroxyproline and removing free radical, at the same time provides its extensive application for making medicine, health-care food, beverage and cosmetic product. When it is used for oral medication, the acceptable daily intake is 10mg-1000 mg, and when it is used for external application, generally it is 0.01%-10%.
WO2005003087A3 Oxazole derivatives as antibacterial agents The present invention provides novel compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel oxazolidinone derivatives of the general formula (I).
EP2094663A2 Pyridine derivatives for the treatment of metabolic disorders related to insulin resistance or hyperglycemia The present invention provides novel compounds represented by the general formula (I): their stereoisomers, pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The invention also relates to a process for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them.
WO2006134494A3 Anti-connexin compounds and therapeutic uses thereof Methods and compositions for modulating the activities of connexins are provided, including, for example, for use for treatment of cardiovascular, vascular, neurological, for wounds and for other indications. These compounds and methods can be used therapeutically, for example, to reduce the severity of adverse effects associated diseases and disorders where localized disruption in direct cell-cell communication or prevention of hemichannel opening is desirable.
WO2002003918A3 Treating neural conditions resulting from spinal cord contusions and other causes β2-agonists, such as clenbuterol and salbutamol can enhance the recovery of locomotive function and/or neuromuscular strength following spinal cord injuries or as a result of degenerative neural conditions such as Mnd. Pharmacological compositions for treating spinal cord injuries and degenerative neural conditions are also provided.
US20120184543 Dihydropteridinone derivatives, preparation process and pharmaceutical use thereof Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
WO2009113910A1 Antiinflammatory and antiallergic gel The invention relates to medicine. The inventive antiinflammatory and antiallergic gel contains N-(β-oxyethyl)-4,6-dimethyldihydropirimidone-2 in a quantity of 3-10 mass% as an active agent, diphenhydramine, or clemastine, or cetiresine in a quantity of 0.005-1.0 mass% as an antihistamine preparation, and a gel base which contains carbopol in a quantity of 0.5-1.0 mass% as a thickener, 0.5-1.0 mass% polyethylenoxide 400-6000 Da, 0-20.0 mass% glycerin, 0.41 mass% ethyl alcohol, the rest being filtered water.
US20100088778 Methods of Treatment, and Diagnosis of Epilepsy by Detecting Mutations in the SCN1A Gene A method for the diagnosis of an epilepsy syndrome, including SMEI or an SMEI-related syndrome, in a patient comprising testing for an alteration in the SCN1A gene in a sample obtained from the patient; and if an alteration is identified, comparing said alteration to any one of those listed in Table 3, wherein if said alteration is identical to any one of those listed in Table 3, a diagnosis of an epilepsy syndrome, including SMEI or an SMEI-related syndrome, in said patient is made in accordance with the correlation set forth in Table 3.
CN102847156A Fatty acid synthase inhibitor and application thereof The invention relates to a fatty acid synthase inhibitor which is prepared by being extracted from natural plant or being chemically synthesized. The fatty acid synthase inhibitor comprises at least one compound shown in the specification, wherein substituent group R of bit 3' can be independently -H or -OH. The fatty acid synthase inhibitor can be applied to preparing a weight-reducing medicine, a medicine for treating cancer, health-care food and functional cosmetics.
EP1461036A4 Bis hydrochloride monohydrate salt of rsv fusion inhibitor The novel crystalline bis hydrochloride monohydrate salt having the formula (II) and pharmaceutical dosage forms thereof is provided having use in the treatment of respiratory syncytial viral infection.
US20070270463 such as N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-quinol-6-ylmethylsulfonamide; azeotropic distillation, crystallization; central nervous system disorders The present invention relates to a novel method for the preparation of azetidine derivatives such as N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-quinol-6-ylmethylsulfonamide and the dihydrochloride thereof and N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide.
EP2197851A1 Derivatives of n-phenylacetamide as inhibitors of the enzyme soat1 for pharmaceutical and cosmetic use The present invention relates to compounds of Formula (I): as well as the cosmetic and pharmaceutical compositions containing such a compound.
US20090162413 Compositions and methods of administering rapamycin analogs with paclitaxel using medical devices Systems and compositions comprising paclitaxel and a second drug, such as rapamycin, analogs, derivatives, salts and esters thereof are disclosed, as well as methods of delivery wherein the drugs have effects that complement each other. Medical devices comprising supporting structures capable of including or supporting a pharmaceutically acceptable carrier or excipient, which carrier or excipient can contain one or more therapeutic agents or substances, with the carrier preferably including a coating on the surface thereof, and the coating including the therapeutic substances, such as, for example, drugs. Supporting structures for the medical devices that are suitable for use in this invention include coronary stents, peripheral stents, catheters, arterio-venous grafts, by-pass grafts, and drug delivery balloons used in the vasculature. These compositions and systems can be used in combination with other drugs, including anti-proliferative agents, anti-platelet agents, anti-inflammatory agents, anti-thrombotic agents, cytotoxic drugs, agents that inhibit cytokine or chemokine binding, cell de-differentiation inhibitors, anti-lipaedemic agents, matrix metalloproteinase inhibitors, cytostatic drugs, or combinations of these and other drugs.
EP2575474A1 Methods for increasing the production or activity of catalase Methods and compositions for increasing the production or activity of catalase in an animal are disclosed. The methods comprise administering vitamin D to the animal in an amount effective to increase catalase production or activity. Methods for treating catalase deficiency, extending the prime years of an animal's life, promoting health and wellness of an animal, and improving the quality of life for an animal through the vitamin D-mediated increase in catalase production or activity are also disclosed. Methods of screening for vitamin D mimetics based on their ability to increase the production or activity of catalase in cells in a manner similar to vitamin D are also disclosed.
US20130012517 Quinoline and Quinoxaline Derivatives as Kinase Inhibitors A series of quinoline and quinoxaline derivatives, substituted by an optionally substituted bicyclic heteroaryl moiety consisting of two fused six-membered aromatic rings attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
CN1850061A Use of triethylene-tetramine as antitumour auxiliary drug The present invention provides a new application of triethylene tetramine as auxiliary medicine for resisting tumor. It uses the triethylene tetramine as telomerase inhibitor and can be matched with other conventional antitumor medicines including doxorubicin, carboplatin and taxol, etc. for curing and preventing tumor diseases.
CN1957945A Glycosyl hyperbranched suppressor in use for anti IIIV adhesion A superbranched glycosylated adhesion inhibitor for HIV is a tree-shaped polymer based on amino kernel or ethyldiamine kernel of glycosylated polyamide-amine polymer, or a tree-shaped polymer of poly (propeneimine).
WO2010111665A1 Methods for preventing major adverse cardiovascular events with dpp-iv inhibitors The present invention relates to methods for preventing or reducing the risk of mortality by any means including, but not limited to, cardiovascular events in mammals, particularly humans, comprising administering a dipeptidyl peptidase 4 (DPP-IV) inhibitor to the mammal or human. In addition, the present invention relates to methods for preventing or reducing the risk of non- fatal myocardial infarction and/or non- fatal stroke in mammals, particularly humans, comprising administering a DPP-IV inhibitor to the mammal or human.
WO2006101062A1 Process for producing carbapenem derivative having 1-alkylpyrrolidine structure A synthetic pathway to produce carbapenem antibacterial agents at low cost with high safety, which pathway is suitable for mass production thereof. There is provided a process for producing carbapenem antibacterial agents with the use of amine compound (1) or salt thereof as a production intermediate: wherein R1 is a C1-C3 alkyl; n is 0, 1 or 2; A is a C1-C3 alkylene; L is an eliminable group; and R3 is a hydrogen atom, a C1-C3 alkyl or an amino protective group, provided that the hydroxyl and carboxyl each independently may be protected.
CN102766080A Pyrrolidine derivative, its preparation method and application thereof The invention discloses a pyrrolidine derivative as shown in the formula I, its preparation method and an application thereof, wherein n is 1 or 2; R1 is C2-C4 alkyl group, 1-3 C3-C6 naphthenic base substituted C1-C3 alkyl group or 1-3 C1-C3 alkoxy substituted C2-C4 alkyl group; R2 is C6-C10 aryl group or 1-2 halogen atom substituted C6-C10 aryl group; and R3 is a phenyl group, 1-2 halogen atom substituted phenyl group, C5-C6 heteroaryl group, 1-2 halogen aatom substituted C5-C6 heteroaryl group or 1-3 C5-C6 heteroaryl substituted C1-C3 alkyl group. The pyrrolidine derivative and its pharmaceutically acceptable salts can have a triple reuptake inhibition effect on a 5-HT/DA/NE transporter, are used to prepare antidepressant drugs, can be used to shorten the onset time, enhance curative effects and minimize side effect, provide a novel approach for preventing and treating depression, and have a better application prospect.
WO2013102929A4 Novel compounds for treatment of diabetes, obesity or related disorders The present invention relates to compounds of the general Formula I their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, their N-oxide, metabolites, polymorphs, use of these compounds in medicine and the intermediates involved in their preparation.
CA2817071A1 Treatment of addiction and impulse-control disorders using pde7 inhibitors This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.
EP1858556A1 Vehicle for topical delivery of anti-inflammatory compounds The present invention relates to a vehicle for topical delivery of a pharmaceutically active ingredient such as anti-inflammatory drugs, comprising a liquid eutectic mixture containing a hydrophobic component. The eutectic mixture comprises, for example, compounds selected from camphor, menthol, thymol, resorcinol, phenol or substituted phenol derivatives. The invention also relates to a method for increasing the solubility of said pharmaceutically active ingredient.
US7429579 antagonism/inhibition, of the D3 receptor; substance abuse. The invention provides compounds of formula (I): wherein: R2 and R3 independently represent various substituents; R1 and R4 independently represent H, F, Cl, Br, C1-2alkyl, C1alkoxy, OH, CN, or NO2; B represents a sulfur atom or a —CH2-group; t represents 3 or 4; and A represents an optionally substituted 5- or 6-membered aromatic heterocyclic ring, or an optionally substituted bicyclic heterocyclic ring system in which at least the ring bound to the group B in Formula (I) is aromatic; or a salt thereof. Preferably, A is selected from one of the groups (i), (ii) or (iii): wherein X1 and X2 are independently N or CR8, and X3 is NR8, O or S; Y1 and Y3 are independently N or CR9, and Y2 is NR9, O or S; Z1 is NR10, O or S, and Z2 and Z3 are independently N or CR10; R8, R9, and R10 are as herein defined, and R7 is H, a halogen atom, OH, cyano, nitro, C1-4alkyl, C1-4alkoxy, C1-4alkylenedioxy, C1-4alkanoyl, or C1-4alkylsulfonyl, an optionally substituted 3-, 4-, 5- or 6-membered cycloalkyl ring, or a group of the formula (a), (b), (c) or (d) as defined by the formulas (a), (b), (c) or (d). The compounds are modulators of dopamine D3 receptors and have potential in the treatment of psychotic conditions (e.g. schizophrenia) or substance abuse.
EP1727819A1 Novel dichloro-phenyl-pyrido¬2,3-d|pyrimidine derivatives, their manufacture and use as pharmaceutical agents The invention describes compounds of the general formula (I), a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. The said compounds show activity as protein kinase inhibitors, in particular src family tyrosine kinase inhibitors, and may therefore be useful for the treatment of diseases mediated by said tyrosine kinases.
WO2014140510A1 Pro-drug compounds A compound according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: wherein where the integers Q, R2, A, R1, Z1, Z2, and Z3 are as defined in claim 1.
WO2014132134A1 A composition comprising a lipid compound, a triglyceride, and a surfactant, and methods of using the same Compositions comprising 2-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenyloxy)butanoic acid, an ester derivative, or a pharmaceutically acceptable salt thereof; a triglyceride; and a surfactant, as well as methods for their use. The present disclosure further relates to self-emulsifying drug delivery systems, such as SEDDS, SMEDDS, or SNEDDS comprising 2-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenyloxy)butanoic acid.
EP2162455A2 Pyrrolopyridine compounds, process for their preparation, and their use as medicaments The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
US20090149472 Salts of substitutted pyrazoline compounds, their preparation and use and medicaments The present invention relates to salts of substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
US20120009170 METHOD OF TREATING INFLAMMATORY LUNG DISEASE WITH SUPPRESSORS OF CpG OLIGONUCLEOTIDES The present disclosure relates to oligodeoxynucleotides that suppress an immune response. Methods are disclosed for inhibiting or treating inflammatory lung disease by administering a therapeutically effective amount of a suppressive oligodeoxynucleotide.
CA2356422C Combinations of ileal bile acid transport inhibitors and cholesteryl ester transfer protein inhibitors for cardiovascular indications The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include an ileal bile acid transport inhibitor combined with a cholesteryl ester transfer protein (CETP) inhibitor.
CN101254199A Panax saponin Rg1 and thein combination and uses thereof The invention relates to a composition comprising ginsenoside Rg1 and caffeine with antifatigue, memory improving and central exciting effects and an application thereof. The composition comprises the following raw ingredients (wt %): ginsenoside Rg1 1-99 and caffeine 99-1. The reasonable formula of ginsenoside Rg1 and caffeine overcomes the shortcoming of caffeine that can only resist short-term sports fatigue, and takes synergistic antifatigue, memory improving and central exciting effects. The inventive composition can be mixed with proper pharmaceutical or food adjutants to prepare into pharmaceutically-acceptable preparations or food preparations.
CN102144962A Powdered osletamirvir phosphate medicinal composition The invention provides a powdered osletamirvir phosphate medicinal composition. The composition comprises osletamirvir phosphate with effective quantity for treatment or prevention, sodium alginate and optional one or more pharmaceutically acceptable excipients. The invention also provides an application of the solid medicinal composition in preparing an oral liquid medicament. The invention further provides a liquid medicinal composition, which comprises the solid medicinal composition and a water-bearing medium. The solid medicinal composition has a stable and excellent effect after being prepared into a suspension with water.
US8809313 Substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes useful for treating HCV infections The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D (Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
EP2050737A1 Mono-and divalent salts of n-(5-hydroxynicotinoil)-l-glutaminic acid exhibiting psychotropic (antidepressant and anxyolytic), neuroprotective, heroprotective and cerebroprotective action The invention relates to medicine, in particular to mono-and divalent salts of N-(5-hydroxynicotinoil)-L-glutaminic acid exhibiting psychotropic antidepressant, anxyolytic, heroprotective, neuroprotective, antihypoxia cerebroprotective and nootropic action. The novel compounds differ from the known preparations, including the closest prior art in the form of a N-(5-hydroxynicotinoil)-L-glutaminic acid base (nooglucotyl), in that they produce psychotropic effects, namely antidepressant, anxyolytic, neuroprotective and heroprotective actions, in such a way that lesion focuses caused by apoplectic attacks are reduced and age-specific neurological deficiencies and intellectual and physical work capacities are improved.
CN102151277A Application of fulvestrant in preparing antimicrotubular chemotherapeutic drug resistance reversal agent The invention provides application of fulvestrant in preparing an antimicrotubular chemotherapeutic drug resistance reversal agent. The fulvestrant reverts antimicrotubular chemotherapeutic drug resistance of breast cancer cells without relying whether estrogen receptors are expressed or not and also without relying whether the function of restricting P-glycoprotein is achieved or not. The fulvestrant and the antitumor drugs which are used together can accelerate the antitumor drugs to induce apoptosis of drug-resistance cells of breast cancer with negative estrogen receptors. The fulvestrant has been approved to be used for clinics and has the advantages of less side effects, good tolerance of a patient, less cross drug resistance with other estrogen receptor regulators or chemotherapeutic drugs, and the like, has clinical operability while being collaboratively used with common chemotherapeutic drugs for clinically treating the breast cancer, such as taxol, adriamycin, vinorelbine, and the like and has favorable clinical application prospect as the antimicrotubular chemotherapeutic drug resistance reversal agent for treating the drug-resistance breast cancer.
US20100197681 Triazolopyridine Compounds and Their Use as Ask Inhibitors The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatory diseases, cardiovascular diseases and/or neurodegenerative diseases and a process for their preparation.
CN103432133A Use of nuclear receptor binding agents The invention relates to use of nuclear receptor binding agents. Concretely, the invention relates to use of a compound, or its optical isomer, pharmaceutically acceptable salt, pharmaceutical product, N-oxide, hydrate or any combination thereof, represented by the structure of Formula VI in preparing medicines for treating, delaying onset, reducing the incidence of, or reducing the severity of a fatty liver condition in a subject.
US20080255080 Hydroquinone Ansamycin Formulations Pharmaceutical compositions of hydroquinone geldanamycin analogs, and uses of such compositions, are provided.
EP1718628A1 Cinnamic amides, process for their preparation, and pharmaceutical compositions containing them E-cinnamic amides of piperazine derivatives according to formula (I) wherein X is chloro or Fluor and R1 is an aromatic or heteroaromatic group. Their pharmaceutically acceptable salts, pharmaceutical compositions containing them and their use in therapy for treating inflammatory, autoimmune, proliferative or hyperproliferative diseases.
CN101347453A Application of attapulgite in pharmacy The invention relates to a novel usage of an attapulgite, which is used for patients with chronic renal failure. After oral administration, the attapulgite can absorb and fix various toxins and metabolic products in the alimentary tract and then discharge out of the body along with intestinal peristalsis, thus reducing or avoiding body injuries and having alimentary hemodialysis, high curing effect and no toxicity and side effect.
EP1141278B1 Therapeutic pde4d phosphodiesterase inhibitors This patent describes the invention of a series of novel therapeutic oligonucleotide polymers targeted at inhibiting expression of genes coding for Phosphodiesterase 4. They are useful as analytical tools in the study of individual PDE isoforms and in the therapeutic treatment of depression, thrombosis, cystic fibrosis, gastric lesions, pulmonary hypertension, glaucoma, multiple sclerosis, atopic dermatitis, asthma and other allergic disorders as well as other illnesses in which an increase of cyclic AMP or a decrease in phosphodiesterase levels is useful.
US20120129838 Composition for Preventing and Treating Alopecia Disorder Containing Morgalanthamine Compounds as an Active Ingredient Provided are a pharmaceutical composition, a cosmetic composition and health foods for preventing and treating alopecia disorder, which include a norgalanthamine compound as an active ingredient. Since the norgalanthamine compound has an effect on growth and proliferation of dermal papilla cells that play an important role in hair growth, the norgalanthamine compound may be used for the pharmaceutical composition, the cosmetic composition and health foods, which are useful in preventing and treating alopecia disorder.
EP2499123A1 Anti-inflammatory compounds New clerodane compounds isolated from plant material from Dodonaea polyandra are disclosed. The compounds have anti-inflammatory activity. Pharmaceutical and cosmetic compositions containing the compounds, as well as methods of treating inflammation using the compounds, are also disclosed.
WO2012022740A1 Combination treatment of multiple sclerosis The present invention is related to the use of Vitamin D in combination with Interferon-beta for the treatment of multiple sclerosis.
CN101062188A Plaster for treating heat and liver disease The invention discloses an externally used medicinal plaster for treating high blood pressure, coronary disease, angina pectoris, diabetes and hepatic diseases, wherein the medicament is prepared from selfheal, cassia seed, capsule of weeping forsythia, clerodendroa cyrtophyllum, natural indigo, subprostrate sophora root, root bark of tree peony, alkanna tinctoria, root bark of chinese wolf berry, mother-of-pearl, magnetite, soybean oil and common resin.
US20090286758 Substituted n-phenyl-5-phenyl-pyrazolin-3-yl amides as cannabinoid receptor antagonists/inverse agonists useful for treating obesity The present invention provides novel pyrazolines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.
CN102068432A Externally applied compound composition consisting of tadines and leukotriene antagonist The invention relates to an externally applied compound composition consisting of tadines and a leukotriene antagonist, wherein the tadines are preferably loratadine and salt thereof; and the leukotriene antagonist is preferably montelukast and salt thereof. The externally applied compound composition can be prepared into externally applied preparations such as nasal drops, eye drops, eye ointments, ointments, gel, inhalants, patches and the like. The externally applied compound composition can be used for local treatment for allergic diseases, can quickly improve allergic symptoms, and has the characteristics of high efficiency, safety, convenient use and the like.
EP2727649A1 Copper-and-titanium-containing composition and production method therefor The Cu- and Ti-containing composition of the present invention contains titanium oxide including rutile-crystal-type titanium oxide, and a divalent copper compound, wherein the rutile-crystal-type titanium oxide exhibits the most intense diffraction peak attributed to rutile-type titanium oxide having a full width at half maximum of 0.65° or less, in a Cu-Kα line X-ray diffraction pattern, which is obtained by plotting intensity of diffraction line with respect to diffraction angle 2θ. The composition exhibits excellent anti-viral property under light and in the dark, and excellent organic compound degradability under light.
CN101817817A Rare earth metal complexes using orbifloxacin as ligand, method for synthesizing same and application thereof The invention discloses rare earth metal complexes using orbifloxacin as a ligand, a method for synthesizing the same and application thereof. In the tests of the inhibiting effect of the complexes on bacteria such as salmonella pullorum, swine streptococcosis and bovine streptococcus uberis, the results show that the complexes have quite high bacteriostatic activity, wherein all of Er(III), Sm(III) and Eu(III) complexes of the orbifloxacin have certain bacteriostatic activity on the swine streptococcosis which cannot be inhibited by orbifloxacin and doxycycline. Mouse acute toxicity tests show that the complexes have low in-vivo toxicity to mice and are highly tolerable to mice. The toxicity of various complexes meets the acute oral toxicity ungraded standards of European Community and the PRC food security assessment grade-two (actually non-toxic) standard, wherein the neodymium complex of the orbifloxacin has the lowest toxicity.
CN101095764B Health-care food having assisted function of treating female urinary tract taint The invention relates to a health-care food that can help treat urinary tract infection for woman, which is characterized in that it takes cranberry juice cocktail extract and grape seed extract as main raw material, and also comprises starch, vitamin C and crystalline cellulose as adjuvant material. Said powder extract and adjuvant material are mixed together and used to produce capsule. The proportion by weight of said raw material is as follows: cranberry juice cocktail extract 5-10, grape seed extract 1-5, starch 1-10, vitamin C 0.1-0.5, and crystalline cellulose 0.1-0.5. The effective component from cranberry juice cocktail extract and grape seed extract can inhibit bacteria from attaching on urinary tract and prevent bacterial growth in human body; the anti-oxidation effect of grapeseed extract is 20 times stronger than that of vitamin C, and it can improve human immunity and promote prevention and treatment effect. The invention is characterized by reasonable formulation, simple preparation process and distinctive health-care effect.
CN101249072A Method for preparing liposomes containing soya bean lecithin rhodiola rosea glycosides with melting method The invention provides a preparation method of salidroside (precursor) liposomes containing soybean lecithin. The method comprises the following steps: mixing salidroside and soybean lecithin at a weight ratio of 1:0.1 to 1:100, heating and melting to obtain a lipid liquid, mixing the lipid liquid with an aqueous solution containing a proppant, cooling, performing reverse phase evaporation or homogenization under 10-50 MPa to obtain a salidroside liposome dispersion, and freeze-drying or spray-drying the dispersion to obtain soybean lecithin-salidroside (precursor) liposomes. By controlling the additional amount of water before use, liposomes of different drug content are available and can meet the requirements for cosmetic formulations. The salidroside (precursor) liposomes containing soybean lecithin have good stability and skin penetrability.
US20100218265 Immune system mediator The present invention discloses an isolated nucleic acid molecule encoding an ISRAA polypeptide comprising a nucleotide sequence exhibiting at least 70% homology to the sequence represented by the nucleotide sequence SEQ ID No: 1. Also disclosed is a recombinant expression vector comprising said nucleic acid molecule and an isolated polypeptide molecule encoded by said nucleic acid molecule.
CN101209995A 5-amidopyrazole derivatives, preparation method and use thereof The invention relates to a 5-amidine pyrazole derivative and a preparation method and application thereof, in particular to a compound that has a structure in formula I or salt that is acceptable in pharmacy of the compound and a preparation method thereof, and the application thereof as medicines, especially as antivirus and antisepsis medicines. Definitions of varied groups refer to the specification.
US20080076808 Pet food of specific dosage of pantothenic acid, nicotinamide, histidine, inositol and choline; treating and preventing skin disorders The present invention provides a composition preferably a pet foodstuff comprising pantothenic acid, nicotinamide, histidine, inositol and choline wherein pantothenic acid is provided at a level of 10 mg to 500 mg per 400 kcal per day, its use in the treatment of a skin disorder and methods of controlling a skin disorder. The invention further provides a method of manufacturing a composition of the invention.
US20110212977 P70 s6 kinase inhibitor and mtor inhibitor combination therapy The present invention provides a combination therapy comprising the compound 4-[4-[4-(4-fluoro-3-trifluoromethyl-phenyl)-1-methyl-1H-imidazol-2-yl]-piperidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine, or a pharmaceutically acceptable salt thereof, and an mTOR inhibitor for use in the treatment of glioblastoma multiforme, adenocarcinomas of the colon, non-small-cell lung cancer, small-cell lung cancer, cisplatin-resistant small-cell lung cancer, ovarian cancer, leukemia, pancreatic cancer, prostate cancer, mammary carcinoma, renal cell carcimoma, multiple myeloma, Kaposis Sarcoma, Hodgkins lymphoma, lymphangioleiomyomatosis, Non-Hodgkins lymphoma or sarcoma.
US20110003777 Methods of Treatment Employing Prolonged Continuous Infusion of Belinostat The present invention relates generally to the treatment of diseases and disorders that are mediated by histone deacetylase (HDAC), for example, cancer, with Belinostat™ (also known as (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide; PXD101; and PX 105684), and more particularly, to improvement treatments of such diseases (for example, cancers, for example, leukemias), which employ prolonged continuous infusion (e.g., prolonged continuous intravenous infusion) of Belinostat™.
CN101279967B Medicinal composition of trimethyl xanthone-4-acetic acid for treating cancer and use thereof The invention relates to a medicine combination, in particular to a medicine combination of trimethyl-genicide-4-acetic acid to cure cancers. The medicine combination contains effective dosages of trimethyl-genicide-4-acetic acid, pharmaceutically acceptable salt or ester thereof, and effective dosages of anticarcinogenic drug. The medicine combination strengthens the antineoplastic activity of the medicine and is of good effect to cancers due to the synergism of the medical components.
CN103623094A Medication for treating gouty arthritis and preparation method thereof The invention discloses a medication for treating gouty arthritis and a preparation method thereof. The medication is mainly prepared by mixing the following medicine according to a proper weight ratio: radices trichosanthis, vicia amoena, scorpion, epimedium, cape jasmine fruit, tiger bone, and the like. The medication disclosed by the invention has the functions of dispelling wind, eliminating dampness, relaxing tendons, activating collaterals, and stopping pain, takes effect quickly when used for treating the gouty arthritis, has a good curative effect without recurrence.
US20130035338 Eyelid treatment The current application is directed topical treatments that improve facial appearance by causing eyelids to naturally open more widely, or be more fully raised, as well as to treatment of ptosis and other eyelid-related conditions. These topical treatments include one or more of travoprost, dorzolamide hydrochloride, timolol maleate, unoprostone, latanoprost, bimatoprost, and related compounds currently used for treating glaucoma and ocular hypertension.
EP2135614A1 Intestinal dismicrobism compound having anti-diarrhoea, anti-inflammatory and lactose and lactose derivative intolerance lenitive properties The present invention relates to an intestinal dismicrobism compound having anti-diarrhoea, antiinflammatory and lactose and lactose derivative intolerance lenitive properties which comprises a prebiotic matrix, constituted of organic and inorganic nourishing substances, and a probiotic matrix, containing bacillus coagulans bacteric cells.
US20080044414 IL-1beta binding antibodies and fragments thereof An IL-1β binding antibody or IL-1β binding fragment thereof comprising the amino acid sequence of SEQ ID NO: 2, and related nucleic acids, vectors, cells, and compositions, as well as method of using same to treat or prevent a disease, and a method of preparing an affinity matured IL-1β binding polypeptide. IL-1β binding antibodies or IL-1β binding fragments thereof are provided which have desirable affinity and potency.
US20080206188 polyethylene glycol monomethyl ether or dimethyl ether, polyoxypropylene glycol; for an inflamed epithelium at risk of developing gut-derived sepsis from an intestinal pathogen; labeled package The present invention provides a system for delivering a wide range of chemical and biological therapeutics, including protein therapeutics, via transepithelial routes. The system comprises a high molecular weight polyethylene glycol-like (HMW PEG-like) compound for use with a therapeutic compound. Optionally, the system comprises a composition containing one or more HMW PEGlike compounds and one or more therapeutics, supplemented with a protective polymer such as dextran and/or essential pathogen nutrients such as L-glutamine. Administered alone, the HMW PEG-like compounds also provide therapeutic benefits. Also provided are methods for preventing or treating epithelial diseases, disorders, or conditions, such as an epithelium at risk of developing gut-derived sepsis attributable to an intestinal pathogen, as well as methods for monitoring the administration of HMW PEG-like compounds.
CN102018707A Medicinal composition for treating diarrhea and preparation thereof The invention discloses a composition for treating diarrhea and a preparation thereof, relating to a medicinal composition for stopping the diarrhea. The invention also relates to a preparation of the medicinal composition for stopping the diarrhea. The medicinal composition is mainly prepared from the main raw materials of 1 part of Racecadotril and 0.25-25 parts of berberine hydrochloride as well as 0.01-250 parts of auxiliary materials in proportion. The medicinal composition has scientific and reasonable prescription, and can be used for inhibiting the rise of calcium ion concentration in colon smooth muscle cells and improving the motion functional coordination of the intestinal tract to realize the effect on stopping the diarrhea mainly by inhibiting the activity of enkephalinase and further inhibiting the excessive secretion of water and electrolyte via the Racecadotril, and simultaneously by the stronger bactericidal effect of the berberine hydrochloride on escherichia coli, Streptococcus hemolyticus, Diplococcus pneumoniae and the like.
EP1345946B1 Macroheterocylic compounds useful as kinase inhibitors This invention is directed to macroheterocyclic compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
WO2012125007A3 Methods and compositions for the treatment, prevention, and alleviation of bone and cartilage diseases or injuries and hair loss The present invention provides pharmaceutical compositions, and methods of preparation and use for the treatment, prevention or alleviation of bone and cartilage diseases or injuries and hair loss. The present invention discloses a method and a pharmaceutical composition comprising mesenchymal stem cells, platelets, activating factors and scaffolding materials for the treatment, prevention, or alleviation of bone diseases, bone injuries or hair loss, and a method and a pharmaceutical composition further comprising dexamethasone for the treatment, prevention, or alleviation of cartilage diseases or injuries.
CA2492724C The use of epidermal growth factor as a gastrointestinal therapeutic agent New utilities for epidermal growth factor (EGF) as a gastrointestinal therapeutic agent are described. In particular, EGF is useful in preventing gastrointestinal colonization by pathogens and in promoting weight gain. As such EGF can be used to treat intestinal infections and increase animal production for example in the agriculture or aquaculture industry. EGF is also useful in increasing the intestinal absorption of immunoglobulins. Inhibition of the epidermal growth factor signaling cascade may be used to prevent uptake of toxic or adverse compounds or to promote weight loss. Therefore, the use of an agent that inhibits the activity of epidermal growth factor to decrease the absorption of substance or decrease weight gain is also described.
CN102477014A Preparation method of histamine dihydrochloride The invention relates to an industrial preparation method of officinal histamine dihydrochloride. The preparation method comprises the following steps of: suspending histidine in hexahydrocresol which is used as a reaction solvent; carrying out a decarboxylation reaction at the temperature of 170 DEG C-175 DEG C; and then quantitatively dropwise adding the hexahydrocresol solution containing hydrochloric acid twice so as to synthesize histamine dihydrochloride. According to the invention, the content of the related substances in histamine dihydrochloride is less than 0.5%, and the content of a single impurity in histamine dihydrochloride is less than 0.1%, thus the histamine dihydrochloride completely meets officinal grade; and the preparation method is simple in equipment, easy and simple in process operation and safe and reliable in reaction; and the solvent can be recycled, thus the preparation method is environment-friendly and is beneficial to industrial large-scale production.
CN101926758A Itraconazole suppository The invention relates to an itraconazole suppository, in particular to the itraconazole suppository comprising 0.05 to 20 weight percent of itraconazole and 80 to 99.95 weight percent of matrix. The itraconazole suppository can be used for treating gynecological fungus infection, takes effect rapidly and obviously reduces adverse reactions caused by taking administration of the itraconazole orally.
US20080287538 Antimicrobial Compositions and Methods Antimicrobial compositions, especially those useful when applied topically, particularly to mucosal tissues (i.e., mucous membranes), including, in particular, a fatty alcohol ester of a hydroxycarboxylic acid, alkoxylated derivatives thereof, or combinations thereof. The compositions can also include an enhancer component, a surfactant component, a hydrophobic component, and/or a hydrophilic component. Such compositions provide effective topical antimicrobial activity and are accordingly useful in the treatment and/or prevention of conditions that are caused, or aggravated by, microorganisms (including viruses).
US7544701 Central nervous system disorders; psychological disorders The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
US8288414 Deuterium-enriched lenalidomide The present application describes deuterium-enriched lenalidomide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US6949586 Synergistic composition of trans-tetracos-15-enoic acid and Apocynin and method of treatment for hepatotoxicity The present invention relates to a synergistic hepatoprotective pharmaceutical composition comprising an effective amount of trans-tetracos-15-enoic acid (TCA) and Apocynin (APO), the present invention also relates to a method of treatment for hepatotoxicity in mammals and humans.
US20070015217 Nucleic acid molecules, polypeptides and uses therefor, including diagnosis and treatment of Alzheimer's disease The present invention provides methods and compositions for screening, diagnosis and prognosis of Alzheimer's disease, for monitoring the effectiveness of Alzheimer's disease treatment, and for drug development. Alzheimer's Disease-Associated Features (AFs), detectable by two-dimensional electrophoresis of cerebrospinal fluid, serum or plasma are described. The invention further provides Alzheimer's Disease-Associated Protein Isoforms (APIs) detectable in cerebrospinal fluid, serum or plasma, preparations comprising isolated APIs, antibodies, pharmaceutical compositions, diagnostic and therapeutic methods, and kits comprising or based on the same.
EP2265599B1 Crystal form of phenylaminopyrimidine derivative The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4- methyl-3-(4-pyridin-3yl-pyrirnidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and their use as anti tumor agent in humans. The compound of formula I, also known as AN- 019, is: Formula I (I)
CN103211787A Glipizide film-controlled slow-release pellet capsule The invention relates to a glipizide film-controlled slow-release pellet capsule. A slow-release film of the glipizide film-controlled slow-release pellet utilizes Eurdragit RL 30D as a film-formation material. A pellet core of the glipizide film-controlled slow-release pellet contains sodium carboxymethyl starch having high expansibility, and also contains pharmaceutically-acceptable common excipients for the slow-release pellet, wherein preferably, the excipients comprise microcrystalline cellulose, lactose and sodium dodecyl sulfate, and the pellet core comprises 5 to 20wt% of sodium carboxymethyl starch. The slow-release film comprises Eurdragit RL 30D, triethyl citrate as a plasticizer and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit RL 30D to triethyl citrate to talcum powder is 30: 3: 4 and a film weight increasing ratio is in a range of 17 to 36%. The glipizide film-controlled slow-release pellet comprises the pellet core containing sodium carboxymethyl starch having high water expansibility and thus after absorbing water, the glipizide film-controlled slow-release pellet obviously expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the glipizide film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.
WO2011135276A1 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza- bicyclo [3.2.1]oct-8-yl)[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted- (6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4, 4-disubstituted piperidin-1 -yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula (I) that, inter alia, inhibit 11 β-hydroxysteroid dehydrogenase type 1 (11 β-HSD1 ). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11 β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11 β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
EP1682508A1 Phenyl derivatives as ppar agonists This invention relates to compounds of the formula wherein one of R 5 , R 6 and R 7 is and X 1 , X 2 , Y 1 to Y 4 , R 1 to R 13 and m and n are as defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR´ and/or PPAR± agonists.
CN102875558A 2-chloro-4-substituted-8-nitrobenzofuran [3,2-d] miazines compound, preparation method of compound and application of compound The invention relates to 2-chloro-4-substituted-8-nitrobenzofuran [3,2-d] miazines compound, a preparation method of the compound and application of the compound. A structure of the compound is shown in the specification, a substituent group R in the formula can be halogen atoms, nitro, amino or amido substituent group. 2-chloro-4-substituted-8-nitrobenzofuran [3,2-d] miazines compound uses 5-nitrososalicylaldehyde, acetic anhydride, hydroxylamine hydrochloride, ethyl bromoacetate and the like as raw materials and is synthesized by six steps, and more than tens of compounds are synthesized and can be used for preparing for antineoplastic medicines.
WO2010094977A1 Novel biphenyl compounds useful for the treatment of hepatitis c The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6 and L are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of hepatitis C virus.
US20120184511 Novel Pharmaceutical Composition Comprising a Macrolide Immunosuppressant Drug The invention provides novel pharmaceutical compositions of macrolide immunosuppressants. The compositions comprise a hydrophilic component, a lipophilic component, and an amphiphilic component. Preferably, the compositions are formulated as liquid microemulsion. Furthermore, the invention provides uses of such compositions, such as for the topical treatment of inflammatory and autoimmune diseases. Methods for preparing the compositions are also provided.
EP0966446B1 Bicyclic inhibitors of protein farnesyl transferase The present invention provides compounds of Formula (I). The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).
EP2069345A2 Pyridazine and pyrrole compounds, processes for obtaining them and uses The present invention relates to nonlinear oligopyridazine compounds, to processes for obtaining them, to their uses, and also to their reduction to oligopyrroles and to the uses of the pyridazinylpyrrole and oligopyrrole compounds obtained. The invention relates in particular to the uses as medicaments, in particular for treating pathologies such as cancer, bacterial infections or parasitic infections, and also the uses in the materials, environmental, electronics and optics field.
US20100216807 Heterocyclic compounds as serotonergic and / or dopaminergic agents and uses thereof Novel heterocyclic compounds of formula I: A-B-D Formula I or a pharmaceutically acceptable salt thereof, wherein: A is selected from the group consisting of a moiety having general Formula II and a moiety having general Formula III: B is a moiety selected from the group consisting of: D is a moiety selected from the group consisting of: which exhibit a dopamine receptor (preferably a D4 receptor) and/or a serotonine receptor (preferably 5HTA1 agonistic activity), processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with the dopaminergic and/or serotonergic systems (e.g., sexual disorders, dyskinesia, anxiety) are disclosed.
CN102973535A Probucol controlled-release tablet for treatment of hypercholesteremia and production method thereof The invention discloses a probucol controlled-release tablet which comprises components in parts by weight: 300-600 of probucol, 40-100 of diluent, 150-300 of controlled-release skeleton substrate, 15-40 of adhesive, 5-12 of lubricant and 12-30 of film coating materials. The probucol spansule is used for the treatment of hypercholesteremia, enables medicaments to release slowly in a body, can keep blood concentration stable and improve the compliance of a patient and lower toxic and side effect, and has curative effect of 24 hours by taking only once each day.
EP1272484B1 Benzoamide piperidine compounds as substance p antagonists The present invention relates to certain benzoamide piperidine containing compounds of formula I and related compounds that exhibit activity as NK-1 receptor antagonists, (e.g., substance P receptor antagonists), to pharmaceutical compositions containing them, and to their use in the treatment and prevention of central nervous system disorders, inflammatory disorders, cardiovascular disorders, ophthalmic disorders, gastrointestinal disorders, disorders caused by helicobacter pylori, disorders of the immune system, urinary incontinence, pain, migraine, emesis, angiogenesis and other disorders. (I)
CN102219772A Cortex pseudolaricis acid complex with bioactivity and preparation method thereof The invention discloses a cortex pseudolaricis acid complex with bioactivity and a preparation method thereof, in particular to a complex formed by a cortex pseudolaricis acid compound and antiviral medicines, antifungal medicines and antitumor medicines which are alkaline, a composition preparation and a preparation method thereof. The cortex pseudolaricis acid complex has better effects than the cortex pseudolaricis acid compound in aspects of water solubility, stability and treatment effects on virus infection, fungus infection and tumors, and is lower in irritation and toxicity.
CA2105666C New centrally acting substituted phenylazacycloalkanes A compound of formula (I), or a pharmaceutically acceptable salt thereof wherein n is 0-3; R1 and R2 are independently H (provided only one is H at the same time), -OH (provided R4 is other than hydrogen), CN, CH2CN, 2- or 4-CF3, CH2CF3, CH2CHF2, CH=CF2, (CH2)2CF3, ethenyl, 2-propenyl, OSO2CH3, OSO2CF3, SSO2CF3, COR4, COOR4, CON(R4)2, SO x CH3 (where, x is 0-2), SO x CF3, O(CH2)x CF3, SO2N(R4)2, CH=NOR4, COCOOR4, COCOON(R4)2, C1-8 alkyls, C3-8 cycloalkyls, CH2OR4, CH2(R4)2, NR4SO2CF3, NO2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R3 is hydrogen, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, -(CH2)m-R5 (where m is 1-8), CH2SCH3 or a C4-C8 alkyl bonded to said nitrogen and one of its adjacent carbon atoms inclusive to form a cyclic structure; R4 is independently hydrogen, CF3, CH2CF3, C1-Cg alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, -(CH2)m-R5 where m is 1-8; R5 is phenyl, phenyl (substituted with a CN, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycioalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl), 2-thiophenyl, 3-thiophenyl, -NR6CONR6R7, or -CONR6R7; R6 and R7 are independently hydrogen, C2-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyimethyl, C2-C8 alkenyl or C2-C8 alkynyl; and with the proviso that when R1 is 2-CN or 4-CN, R2 is H, R3 is n-Pr and n is 1 or 3 then such compound is a pure enantiomer. The formula (I) compounds possess selective pharmacological properties and are useful in treating central nervous system disorders related to dopamine receptor activity including depression symptoms, geriatric disorders in the improvement of mental and motor functions, schizophrenia, narcolepsy, MBD, obesitas, and disturbances of sexual functions and impotence.
CN102805873A Gene drug co-carrier system using cation liposome to establish gold nano-spherical shell and preparation method The invention relates to a gene drug co-carrier system using cation liposome to establish a gold nano-spherical shell and a preparation method. The method comprises: using phosphatides such as DPPC, MPPC and DPPE-PEG and the derivatives thereof to form the cation liposome via membrane extrusion; carrying the hydrophilic drug hydrochloric acid adriacin into the liposome in the forming process; forming the drug-carried cation liposome; adding chlorauric acid solution into cation liposome solution; adsorbing on the surface of the cation liposome; adding ascorbic acid solution for reduction; forming the gold nano-spherical shell structure; reducing sulfhydryl out of the single chain of green fluorescent protein silent gene with a disulfide bond, grafting onto the surface of the gold nano-spherical shell; and forming the gene drug co-carrier system. The gold nano-spherical shell has low toxicity and unique optical properties. The gene drug co-carrier system using cation liposome to establish the gold nano-spherical shell can provide carrier for the co-treatment of drugs and genes, can select light to illuminate the gold nano-spherical shell, and utilize light-heat conversion property to realize the co-release of the drugs and genes.
CN1977832A Novel sterile powder injection containing sodium new houttuyfonate orits receivable salt or derivative The present invention belongs to the field of medicine technology, and discloses a new sterile powder injection preparation including new houttuynine sodium bisulfite or its acceptable salt or its derivative and excipient. Its grain size is less than or equal to 100 micrometers. Besides, it also has a special-purpose solvent injection for dissolving said new sterile powder injection preparation.
CN103006628A Application of formaldehyde in preparation of injection for treating animal and human infectious disease The invention discloses a new application of formaldehyde in preparation of an injection for treating animal and human infectious diseases. The content of formaldehyde in the injection for treating different animals and human beings and the medication doses are determined. In Tens of thousands of cases of clinical practice, for the animal infectious diseases including swine fever disease, fowl plague disease, tetanus disease, foot and mouth disease, rabies, swine plague, flu, trypanosomosis, brucellosis, viral enteritis and the like, for the acute diseases, in which body temperature cannot drop naturally, and for the chronic diseases, in which a patient is extremely thin and has no denaturation in a certain organ, the diseases can be recovered by the treatment with the injections once, and the curative effect is definite; and the human infectious diseases, including hepatitis B, hepatitis C, chronic phthisis, acquired immunodeficiency syndrome and the like, can be recovered in 2-3 days.
WO2008064039A3 Prostaglandin prodrugs as ocular hypotensive agents Novel compounds of the following formula, and therapeutic methods, compositions and medicament related thereto are disclosed herein. (Formula) or a pharmaceutically acceptable salt thereof; wherein Y is -CO2(CH2)2OH or (Formula) A is -(CH2)6-, cis -CH2CH=CH-(CH2)3-, or -CH2CΞC-(CH2)3-, wherein 1 or 2 carbon atoms may be substituted with S or O; or A is -(CH2)m -Ar-(CH2)O- wherein Ar is interarylene or heterointerarylene, the sum of m and o is from 1 to 4, and wherein one CH2 may be substituted with S or O; B is C=O, CH2, CHOH, CHC1, CHF, CHBr, or CHCN; G is OH or H; and D is aryl or heteroaryl.
CA2224075C Vectors for the diagnosis and treatment of solid tumors including melanoma The present invention is directed to the isolation and use of super-infective, tumor-specific vectors that are strains of parasites including, but not limited to, bacteria, fungi and protists. In certain embodiments, the parasites include, but are not limited to, the bacterium Salmonella spp., such as Salmonella typhimurium, the bacterium Mycobacterium avium and the protozoan Leishmania amazonensis. In other embodiments, the present invention is concerned with the isolation of super-infective, tumor-specific, suicide gene-containing strains of parasites for use in treatment of solid tumors.
US20060058252 Methods and materials for treating human papillomavirus infections The invention provides methods and materials related to treating HPV infections (e.g., HPV infections of cutaneous and mucosal epithelial cells) and HPV-associated conditions (e.g., cervical dysplasia, HPV-associated cervical carcinomas, oral mucosal papilloma cancers, laryngeal papilloma cancers).
WO2009139362A1 Pharmaceutical preparation comprising dpp-iv inhibitor and other diabetes therapeutic agent in concomitant or combined form Disclosed is a pharmaceutical preparation which is very useful for the treatment of type-2 diabetes, diabetic complications or impaired glucose tolerance. The pharmaceutical preparation is characterized in that a compound represented by general formula (I), a salt of the compound, or a solvate of the compound or the salt and at least one other diabetes therapeutic agent are administered in combination. [In general formula (I), R1, R2, R3 and R4 independently represent a hydrogen atom, a trifluoromethyl group or a C1-3 alkyl group.]
WO2012086857A1 Combination body for photodynamic diagnosis or therapy and a production method therefor The present invention relates to a combination body of an acetylated biocompatible polysaccharide and a phthalocyanine compound for photodynamic diagnosis or therapy, and relates to a production method therefor. More specifically, the invention relates to a combination body for photodynamic diagnosis or therapy in which a biocompatible polysaccharide is subjected to acetylation and a phthalocyanine compound is bound to the acetylated polysaccharide, and relates to a production method therefor. The combination body for photodynamic diagnosis or therapy according to the present invention can be used to advantage in diagnosis or therapy of diseases involving the use of photodynamics. This is because the acetylation of the polysaccharide increases the solubility in solvents and allows various forms of chemical modification, such that it is possible to specifically mark only cancer cells and the specificity for and ability to accumulate in cancer cells is outstanding, and, additionally, there is an outstanding effect whereby cancer cells are killed during near-infrared irradiation while on the other hand no cytotoxicity is exhibited with respect to cells other than cancer cells even during near-infrared irradiation and hence the in-vivo stability is outstanding.
CN103222994A Medicinal or healthcare food composition for improving immune function, and preparation method thereof A medicine or healthcare food for improving the immune function is characterized in that the medicine or healthcare food comprises 2-20wt% of a white fungus extract, 10-60wt% of a Manyprickle Acathopanax Root extract, 2-20wt% of vitamin C, 20-40wt% of microcrystalline cellulose and 0.1-20wt% of magnesium stearate. The production method of the medicine or healthcare food mainly comprises the following steps: taking the above components, precisely weighing, sieving, sequentially adding the white fungus extract, the Manyprickle Acathopanax Root extract and vitamin C to prepare a soft material, adding the microcrystalline cellulose and magnesium stearate, mixing, preparing a soft material, granulating, drying, and granulating. The medicine or healthcare food can activate the immune system and enhance the immune function of the body, removes oxygen radicals in the body and reduces the production of toxic substances in the body through heat clearing and detoxifying, and enhances the drainage of the toxic substances to improve the immune function of the body.
US20120316203 Compositions and Methods for Inhibition of Cancers Methods and compositions for treating cancers, including ovarian cancers, are described. The compositions generally include a redox based curcumin derivative, diarylidenylpiperiden-4-one (DAP) having a hydroxylamine moiety attached thereto.
CN101613362B 3-carbonyl-6-ethoxycarbonyl-thiazole pyrimidine compound and synthesis method and application thereof The invention relates to a 3-carbonyl-6-ethoxycarbonyl-thiazole pyrimidine compound and a synthesis method and application thereof. The compound has a structure formula as below. The 3-carbonyl-6-ethoxycarbonyl-thiazole pyrimidine compound serving as an inhibiting agent of YyCG histidine kinase protein for a staphylococcus epidermidis signal transduction system has a novel structure, and the adopted method for preparing the compound is simple and easy to implement. The test results of the minimal inhibitory concentration (MIC) and the minimal bactericidal concentration (MBC) show that the compound has excellent inhibitory action on the formation of a staphylococcal biological film and can effectively kill and wound the bacteria in the staphylococcal biological film.
CA2801426A1 Combination cancer therapies with wortmannin analogs Provided herein are combination therapies for the treatment of certain cancers in a subject by administering a combination of a therapeutic and a wortmannin analog to that subject.
WO2008077234A1 Synergistic effects of c3, cyclic amp and ciliary neurotrophic factor on neuronal survival and axonal regeneration The present invention relates to the synergistic effects of a combined administration of a Rho antagonist, e.g. a C3 fusion protein, with a growth factor, e.g. CNTF, and cAMP or analogues or modulators thereof, which have synergistic effects on promoting neuronal, e.g. adult RGC survival and axonal regeneration. The present invention relates therefore to compositions, and to methods for treating comprising administering the compositions of the invention to a subject in need thereof, for promoting neuronal, e.g. adult RGC survival and axonal regeneration in a subject. Exemplary compositions of the invention comprise Rho antagonists, e.g. C3 proteins or C3-like proteins, growth factors such as CNTF, and CAMP, or analogues or modulators thereof. It is also provided that the effects of administering SEQ ID NO: 4, CNTF and cAMP or CPT-CAMP are synergistic, increasing both the number of surviving RGCs and the proportion of viable RGCs that regenerate an axon.
CN101822825A Paste for preventing infection of purulent and exudative skin diseases The invention relates to a paste for preventing infection of purulent and exudative skin diseases, which is used for treating the patients infected with purulent and exudative skin disease and inspected during an health examination for workers engaged in the industries including food, public places, cosmetics, drinking water and nursery institution, and for preventing infection of the medical care personnel implementing the health examination. Especially, the paste is most satisfactory in treating the purulent skin disease resulting from purulent staphyloccocus aureus rosenbach and the exudative skin disease from candida albicans, and has a function of eliminating odor.
US20080019919 Method for optimizing cancer therapy by monitoring maturation of tumor associated vasculature by selenium This invention provides a method for a method for optimizing the regimen for the administration of chemotherapeutic agents. The method comprises administration of a selenium compound to an individual, monitoring the modulation of tumor vessel maturation (TVM) to identify an optimal time for administration of a chemotherapeutic agent. This invention also provides a method to determine whether or not a tumor is likely to be a responder to chemotherapy. The method comprises administration of a selenium compound to an individual and determining whether or not an increase in TVM is observed. An increased TVM following administration of selenium is an indication that the tumor will likely respond the chemotherapy.
EP1417196B1 Dna-pk inhibitors The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R?1 and R2¿ are independently hydrogen, an optionally substituted C¿1-7? alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR?4¿ and O, O and CR'4 and NR'4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R?3 and R4 or R'4¿ is an optionally substituted C¿3-20? heteroaryl or C5-20 aryl group, and the other of R?3 and R4 or R'4¿ is H, or R?3 and R4 or R'4¿ together are -A-B-, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.
WO2011112428A3 Arylvinylazacycloalkane compounds for constipation The present invention relates to methods of treating constipation and enhancing colonic motility by administration of 5-((E)-2 pyrrolidin-3-ylvinyl)pyrimidine or a pharmaceutically acceptable salt thereof.
WO2009015844A1 Novel combinations of neramexane for the treatment of neurodegenerative disorders The present invention relates to combinations comprising neramexane and a Glutamate Release Inhibitor (GRI) and the use of such combinations in the treatment of neurodegenerative disorders.
CN103420982A Dabigatran derivative, and preparation method and application thereof The invention relates to a preparation method of a benzimidazole derivative shown as a general formula I, wherein R1, R2 and R3 are defined as in the specification. The invention relates to a Dabigatran derivative shown as the general formula I and non-toxic pharmaceutically acceptable salts thereof, and a pharmaceutical composition containing these compounds as active components, and application of the compounds and the pharmaceutical composition as thrombin inhibitors.
US7208522 Methods and compositions for the prevention and treatment of Syndrome X Methods and compositions for preventing or treating Syndrome X are provided. The method includes administering a therapeutically effective amount of conjugated linoleic acid.
US20080260725 Tag and target delivery system A system for targeting dividing cells and delivering therapeutic agents to the targeted cells using a Tag nanoparticle. Each Tag nanoparticle comprises a nucleotide encoding a Tag, which is expressed only in dividing cells. The system optionally utilizes a microparticle to deliver Tag nanoparticles to cells. Therapeutic nanoparticles comprising therapeutic compounds are subsequently targeted to the tagged cells via surface molecules that specifically bind to the Tag. The system may be adapted for specific patient needs, for example, targeting and eliminating cancer cells, preventing metastasis and secondary tumors, stimulating or inhibiting proliferation of endothelial cells, and stimulating cell regeneration in diseased organs such as liver.
CN101669932B Application of long effective curcumin derivative in preparing anti-depression drug The invention relates to an application of a long effective curcumin derivative in preparing an anti-depression drug. The long effective curcumin derivative is an ester which is formed in such a way that C1 to C50 saturated or unsaturated fatty acids or acyls thereof react with hydroxyl groups of curcumin substances by esterification respectively and independently. Through the research on the anti-depression action of various animal models, the long effective curcumin derivative can reserve the inherent anti-depression drug effect of the curcumin and also has the effects of the slow release and the prolongation of the drug effect and a favorable prospect of clinical application. The long effective curcumin derivative can be also used for preparing anti-depression drinks, foods, food addiitives or health products.
WO2013169337A1 Polymer conjugates with a linker This application relates generally to biocompatible water-soluble polymers with pendant functional groups and methods for making them, and particularly to polyglutamate amino acid conjugates that can include a linker to a compound that can include a drug, and their use for a variety of drug delivery applications, e.g., anticancer.
CN102659844A Cr (III) chelate, and preparation method and application thereof The invention provides a Cr (III) chelate, and a preparation method and application thereof. The preparation method for the chelate comprises the following steps: preparing 5,5-methylene di(2-hydroxybenzoic acid); putting Cr (III) Cl3.6H2O and the 5,5-methylene di(2-hydroxybenzoic acid) into a reactor, dissolving by using organic alcohol, adding zinc particles, dripping ethanediamine in a reflux state, and continuously reacting for 15 to 60 minutes, wherein 1.85g of 5,5-methylene di(2-hydroxybenzoic acid), 0.1 to 1g of zinc particles, 10 to 30ml of organic alcohol and 0.5 to 1g of ethanediamine are added into each 1g of Cr(III)Cl3.6H2O; and cooling and filtering a reaction liquid to obtain a target product. The chelate is high in water solubility, has a sustained release function, is easily absorbed and can be applied to preparing weight-reducing medicines.
EP2467377A2 Substituted benzoazepines as toll-like receptor modulators Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.
US8518896 Treatment of cancers of the blood using selected glycomimetic compounds Methods and medicaments therefor are provided for the treatment of cancers of the blood or a complication therewith in an individual. More specifically, the use of particular glycomimetics for the treatment is described. Methods and medicaments therefor are also provided without regard to cancer type for reducing in an individual the myeloablative bone marrow toxicities of chemotherapy.
US20100184856 Novel Compounds and Uses Thereof for Treating Inflammation and Modulating Immune Responses The present invention provides compounds, and compositions comprising these compounds, which have immunomodulatory activity and/or anti-inflammatory activity.
WO2013150173A1 New alpha2 adrenoceptor agonists Compounds of formula (I), wherein X and R1-R6, are as defined in the claims, exhibit alpha2 agonistic activity and thus useful as alpha2 agonists, especially as alpha2A agonists. Methods of use of said compounds are also provided.
WO2005007069A3 Soft gel formulations for saquinavir The present invention describes a pharmaceutical composition with increased bioavailability, which is suitable for preparing microcapsules for the therapeutic administration of a protease inhibitor. It is also described a process for preparing a pharmaceutical composition with increased bioavailability, suitable to prepare concentrate pharmaceutical compositions comprising retroviral protease inhibitors.
CN101342188A Application of bletilla striata polyoses in preparing medicament for reinforcing hematopoiesis function The present invention relates to the application of white mustard polysaccharide in preparing medicines for enhancing hematopoietic function. The application includes the application of white mustard polysaccharide in preparing medicines for enhancing hematopoietic function, for increasing leucocytes, for increasing hematopoietic stem cells, for increasing erythrocytes and platelets and for curing anaemia.
CN103550778A Pharmaceutical composition for treating affective disorder disease The invention provides a pharmaceutical composition comprising a 5-HT1A receptor stimulant and a mood stabilizer. In the pharmaceutical composition, the weight ratio of the 5-HT1A receptor stimulant to the mood stabilizer is (1-40):(50-800). The invention also provides application of the pharmaceutical composition. Through combination of selective 5-HT1A receptor stimulant and the mood stabilizer which have different action mechanisms, the drug can treat anxiety, depression and/or biphasic emotional disorder and the like at the same time; the disease treatment spectrum is wider; furthermore, the curative effect after combination is more significant than that of single medicine, and the toxic and side effects are lower; a novel drug selection is provided to patients who are intolerant to first-line anti-anxiety or anti-depression or drugs.
CN102766184A Protopanoxadiol peroxide derivatives as well as preparation method and application thereof The invention discloses a protopanoxadiol peroxide derivatives as well as a preparation method and an application of the protopanoxadiol peroxide derivatives. The structural formulae of the protopanoxadiol peroxide derivatives disclosed by the invention are shown in formulae I, II and III. In the method, the microbial conversion technology is utilized to modify structure of protopanoxadiol successfully so as to obtain various novel compounds. In-vitro anti-tumor cell test shows that the compounds have better anti-tumor activity, so that the compounds can be used as active components of the anti-tumor drug and have wide application.
CN101849927A Hot-melt pressure-sensitive adhesive transdermal patch containing alpha-asarone and preparation method thereof The invention discloses a hot-melt pressure-sensitive adhesive transdermal patch containing alpha-asarone, which comprises a back lining, a storage warehouse layer and an anti-sticking layer. The storage warehouse layer is prepared from the following raw materials in percentage by weight: 1-20 percent of alpha-asarone, 70-98 percent of hot-melt pressure-sensitive adhesive and 1-10 percent of transdermal accelerant. The transdermal patch adopts the hot-melt pressure-sensitive adhesive with both hot-melt and pressure-sensitive properties as a base material, has the advantages of no organic solvent and low pollution nuisance; in addition, the preparation of the transdermal patch has the advantages of high coating speed and high degree of automation.
EP1150996B1 New amidinobenzylamine derivatives and their use as thrombin inhibitors There is provided compounds of formula (I) wherein R?1, R2 Y, R3 and R4¿ have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
CA2809028A1 Nicotinic receptor compounds Provided herein are compounds and methods of preparation of compounds that are capable of functioning as agonists or antagonists of a nicotinic receptor. Also provided are pharmaceutical compositions comprising one or more of these compounds, which may further comprise one or more additional therapeutic agents. Further provided are methods of treatment of various conditions that may be responsive to such activity at the nicotinic receptors, such as nicotine dependence.
EP2396316A1 Quinazolinones as prolyl hydroxylase inhibitors Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
US20100035796 17-alpha-substituted derivatives of estradiol with wound-healing activity The invention relates to 17α-(5-hydroxy-C5-hydrocarbyl)-1,3,5(10)-estratrien-3,17β-diol derivatives having cicatrising activity, preferably for topical use on wounds, without significant systemic effects, and to pharmaceutical compositions containing them. In particular, the invention relates to estradiol 17α-(5-hydroxypentyn-1-yl)derivatives and 3-esters, 5′-esters and 3,5′-diesters thereof and to a process for the preparation thereof by reaction of 3-OR-protected estrone with an alkali metal derivative of OR-protected 5-pentynol, followed by 3-, 5-′ or 3,5′-esterification.
WO2007026725A2 Drug, drug gudance system, magnetic detection system, and drug design method A drug comprises an organic or inorganic compound, and is made magnetic by modification of side chains and/or crosslinking between side chains.
WO2010096791A1 (+)-6-hydroxy-morphinan or (+)-6-amino-morphinan derivatives The present invention provides (+)-morphinanium compounds comprising substituted 6-hydroxy or 6-amine groups. The invention also provides methods for inhibiting microglial activation by administering the compounds of the invention.
WO2014025814A1 Treatment regimens The invention further relates to compounds, pharmaceutical compositions and methods for treating all disorders of human sexual function including hypoactive sexual desire disorder (HSDD) in a subject.
US20120157406 Method of preventing diarrhoea The present invention provides a method for the prevention of the incidence of and/or a reduction in the duration of acute diarrhoea, particularly in travellers, said method comprising orally administering an oligosaccharide composition, in particular a non-digestible oligosaccharide, to a mammal.
WO2008157407A3 Thiadiazole, oxadiazole and triazole derivatives for treating leukemia Compounds of formula (I) hat are inhibitors of transcription factors of leukemia cell lines are provided. In addition, pharmaceutical compositions including the inhibiting compounds and methods for treating leukemia are also provided.
US20050059657 Aminoisoxazole derivatives active as kinase inhibitors Compounds (I) which are aminoisoxazole derivatives or pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compositions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.
US20100240601 Coordination Complexes, Pharmaceutical Solutions Comprising Coordination Complexes, and Methods of Treating Patients A coordination complex having a physiologically acceptable pKa includes a metal and a biologically active agent. The pKa of the coordination complex is less than the pKa of the biologically active agent. A pharmaceutical solution for treating a patient includes a coordination complex and water, wherein the coordination complex is at least partially soluble in the water at physiological pH and in a therapeutically efficacious concentration. A method for treating a patient includes administering a pharmaceutical solution including a coordination complex and water to a patient in need of a biologically active agent.
WO2012170867A1 Novel compounds as modulators of gpr-119 The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them.
US20080319025 Therapeutic and Diagnostic Methods Dependent on CYP2A Enzymes A method of regulating the activity of human cytochrome P450 isozyme CYP2A6 to control nicotine metabolism or decrease to production of carcinogens from procarcinogens, such as those present in tobacco smoke, in an individual by selectively inhibiting CYP2A6. Various prophylactic (i.e., prevention and treatment) compositions and methods are also described, including an improved oral nicotine composition and method comprising the use of nicotine together with an inhibitor of the CYP2A6 enzyme. Furthermore, it has been discovered that the presence in an individual of a mutant allele of human cytochrome P450 enzyme CYP2A6 (referred to throughout this specification as “CYP2A6” for brevity) is predictive of an individual who: (i) has a decreased risk of becoming a smoker, (ii) will smoke less if he/she becomes dependent, and/or (iii) may be at relatively lower risk for cancer due to both decreased smoke exposure and decreased CYP2A6-mediated activation of tobacco smoke and other procarcinogenic substrates. This invention provides diagnostic methods for predicting tobacco dependence risk and risk for cancers related to CYP2A6 substrates in an individual by analysing for the presence of a mutant genotype for human cytochrome P450 enzyme CYP2A6 in an individual, ranging from gene duplication (multiple copies of CYP2A6) to single or even no copies due to null alleles or gene deletion.
WO2008081914A1 Novel aminopyrimidine derivative as plk1 inhibitor Disclosed is a compound represented by the general formula (I) below, or a pharmaceutically acceptable salt or ester thereof. (In the formula, R1 and R2 may be the same or different and represent a hydrogen atom, a lower alkyl group, a cycloalkyl group or the like; R3 and R4 may be the same or different and represent a hydrogen atom, a lower alkyl group, an NRaRb, a phenyl group, a lower alkyl group substituted with a phenyl group, a 4- or 7-membered aliphatic heterocyclic group, a lower alkyl group substituted with a 4- or 7-membered aliphatic heterocyclic group, a 5- or 6-membered aromatic heterocyclic group, a lower alkyl group substituted with a 5- or 6-membered aromatic heterocyclic group or the like; and R5 represents a hydrogen atom, a cyano group, a halogen atom or a lower alkyl group.)
US7429573 Osteoporosis A method of treating a mammal for a purpose selected from the group consisting of (a) increasing bone mineral density (BMD), (b) treating low BMD, (c) preventing and treatment of low impact fractures, (d) treatment of high impact fractures; (e) treating osteoporosis; (f) modulating a growth factor that influences bone metabolism; and (g) improving bone micro-architecture or connectivity of bone; the method comprising administering to the mammal an effective amount of a N-acylated-2-glucosamine derivative of the general formula (I): wherein R is an alkyl radical of the general formula CnH2n+1 and n is selected from 2-12; or pharmaceutically-acceptable salts, esters and glucosides thereof; or pharmaceutically-acceptable compositions thereof.
WO2011138797A3 Delayed release oral disintegrating pharmaceutical compositions of lansoprazole The present invention relates to delayed release oral disintegrating pharmaceutical compositions of lansoprazole or pharmaceutically acceptable salts thereof. The invention also relates to processes for the preparation of such compositions.
CN101036787A The application of medicine composition containing proton pump inhibitor in the novel gastroenteritic compound capsule and the preparation The invention relates to a preparation and application of drug combination containing proton pump inhibitor in new type gastrointestinal complex capsule, belonging to pharmacy domain. The drug combination comprises proton pump inhibitor of medicinal dose or stereoisomer thereof and salt thereof used as medicine, gastrointestinal motility-drug of medicinal dose, or salt thereof used as medicine or carrier or excipient thereof used as medicine.
US6943186 Administering benzopyrazolyl compound for therapy of sepsis The present invention features a method for treating sepsis. The method includes administrating to a subject in need thereof an effective amount of a fused pyrazolyl compound of formula (I): A is H, C1˜C6 alkyl, or in which n is 0, 1, 2, or 3; each of Ar1, Ar2, and Ar3, independently, is phenyl, pyridinyl, thienyl, furyl, or pyrrolyl; and each of R1, R2, R3, R4, R5, and R6, independently, is XYZ; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)1-6O; in which X is a bond or C1˜C6 alkylene, Y is a bond, O, S, OC(O), OC(O)(CH2)1-6C(O)O, C(O)O, C(O)S, C(O)NH, C(O)NC1˜C6 alkyl, NH, or NC1˜C6 alkyl, and Z is H, halogen, CN, NO2, or C1˜C6 alkyl; and provided that one of R3 and R4 is not H.
EP0986551B1 Sulfonamide derivatives, their production and use The present invention provides compounds which specifically inhibit FXa, which are effective when orally administered and which are useful as a safe medicine for the prevention or treatment of diseases caused by thrombus or infarction. Compounds of this invention are piperazinones of formula (I), wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, in addition to the group of formula (II) and the group of formula (III); Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent heterocyclic group; X is a direct bond or an optionally substituted alkylene chain; Z is: (1) an amino group substituted with an optionally substituted hydrocarbon group, (2) an optionally substituted imino group or (3) an optionally substituted nitrogen-containing heterocyclic group; provided that when X is a direct bond and Z is an optionally substituted 6-membered nitrogen-containing aromatic heterocyclic group, Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent unsaturated heterocyclic group; or a salt thereof.
US20080262076 Novel Tetracyclic Tetrahydrofuran Derivatives Containing Cyclic Amine Side Chain This invention concerns novel substituted tetracyclic tetrahydrofuran derivatives containing a cyclic amine side chain with binding affinities towards dopamine receptors, in particular dopamine D2 receptors, towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein all substituents are defined as in Claim 1.
CN102716154A Processing method and product of ionized calcium water-solubility preparation A processing method of an ionized calcium water-solubility preparation includes: preparing 90 kilograms of oyster shells, 70 kilograms of pearl shells, 3 kilograms of corallites, 50 kilograms of stalactite, 5 kilograms of pearl powder, 30 kilograms of keel, 5 kilograms of dens draconis, 50 kilograms of haliotis, eggshells and 50 kilograms of other shells; grinding dirt and impurities on the surfaces of the raw material shells, performing cleaning and screening, and crushing the shell raw materials; and smashing other non-shell raw materials. The processing method and the product of the ionized calcium water-solubility preparation aim at being capable of regulating acid-base balance of human body, can replenish various trace elements and mineral substances required by human bodies, enable food to be better in taste, can retain freshness of food, remove pesticide residue and hormone residue in foods, remove abnormal flavor on articles and are good in anti-alcohol effect.
US20080176874 Derivatives of Pyrido[2,3-d]pyrimidine, the Preparation Thereof, and the Therapeutic Application of the Same The invention relates to derivatives of pyrido[2,3-d]pyrimidine, to the preparation thereof, and to the therapeutic application of the same.
WO2011161151A1 Use of dibenzofuranone derivatives to inhibit kinases The invention relates to a pharmaceutical product comprising a dibenzofuranone derivative as the active ingredient. The invention further relates to the use of dibenzofuranone derivatives to inhibit kinases, in particular serine/threonine kinases, to the use of dibenzofuranone derivatives for producing drugs and/or medicinal products for treatment, and to the use of dibenzofuranone derivatives as a diagnostic product for analyzing the role of protein kinases, in particular serine/threonine kinases, in particular protein kinase CK2 in cellular processes, the pathogenesis of diseases, ontogenesis and/or other developmental biological phenomena or relationships.
CN102895670A Water-soluble molecular target porphin photosensitizer and preparation method thereof The invention relates to a water-soluble molecular target porphin photosensitizer and a preparation method thereof. The photosensitizer is characterized in that the two bridged ends of polyethylene glycol (PEG) diamine are respectively connected with folic acid and porphin with substituent groups, wherein other substituent groups can be connected with the porphin, and the average molecular weight of PEG is 1000-10000. According to the preparation method of the water-soluble molecular target porphin photosensitizer, PEG diamine reacts with folic acid so as to produce PEG amine which is obtained from single folic acid, and the PEG amine has amidation with carboxyl, acyl chloride or anhydride substituent group on the porphin so as to obtain the porphin-PEG-folic acid target photosensitizer. The photosensitizer has good photodynamic activity, tumor target performance and good water solubility and is applicable to intravenous administration; the phagocytosis of macrophage to the photosensitizer can be reduced, the body circulation time of the photosensitizer is prolonged and the bioavailability of the photosensitizer is improved. Moreover, the preparation method of the water-soluble molecular target photosensitizer is simple to operate, has moderate conditions and has strong repeatability.
CN101259103A Camptothecinum derivative emulsion agent and preparation thereof The invention provides an emulsion of camptothecin derivative which comprises the components by weight: 0.01 to 0.1 percent of 10-methyl-9 nitryl camptothecin, 5 to 20 percent of oil for injection, 1-4 percent of emulsifier, 1-4 percent of co-emulsifier, 0 to 60 percent of solubilizer, 2 to 3 percent of glycerin of isotonizing agent and Vitamin E and the rest is water for injection; the sum of the percentages of all components is 100 percent. The emulsifier and a co-surfactant are dissolved in the oil for injection, heated and added with the solubilizer and 10-methyl-9 nitryl camptothecin to be dissolved, ant then added with the glycerin of isotonizing agent and the water for injection and made into primary emulsion by means of high speed homogenization or ultrasound, then further made into the emulsion by means of high pressure homogenization or micro jet. The prepared emulsion of the invention has uniform particle diameter and high content of drug and the appearance of the emulsion is a milky white or blue opalescence homogeneous system; meanwhile, compared with other preparation methods, the micro jet technique is adopted by the invention to prepare the emulsion, so as to ensure less loss of drug and better stability of the emulsion. The emulsion of camptothecin derivative of the invention has reasonable design and easy operation, which is suitable for practical use.
CN101700342A Pharmaceutical composition for treating hepatitis B and preparation method thereof The invention discloses a pharmaceutical composition for treating hepatitis B and a preparation method thereof. The pharmaceutical composition is prepared by the following components: ganoderma lucidum polysaccharide, radix tetrastigme, disporopsis fuscopicta, radix bupleuri and the like. The preparation method comprises the following steps: weighing the raw materials according to the formula ratio; grinding the above raw materials into coarse powder except for ganoderma lucidum polysaccharide; decocting with water twice, wherein, the first decocting lasts 3h, and the second decocting lasts 2h, filtering, concentrating the filtrate into thick paste; drying, pulverizing; sieving with a 100 meshes sieve; adding ganoderma lucidum polysaccharide; evenly mixing, moistening, softening, and taking out agglomerated product to obtain medicinal granules. The compound preparation prepared by the method of the invention adopts oral dosage form, has convenient use and good mouth feel, is easy to accept by the patients, and has strong function of inhibiting and removing hepatitis B virus, and the negative conversion ratio of HBsAg can reach over 58% after the patient takes the pharmaceutical composition for 6 months; the compound preparation has low treatment cost and can save over 68% of cost compared with the conventional treatment.
US7902399 Fatty acids analogous The present invention relates to novel fatty acid analogous of the general formula (I): R1—[xi—CH2]n—COOR2 wherein R1 is: a C6-C24 alkene with one or more double bonds and/or with one or more triple bonds, and/or a C6-C24 alkyne, and/or a C6-C24 alkyl substituted in one or several positions with one or more compounds selected from the group comprising fluoride, chloride, hydroxy, C1-C4 alkoxy, C1-C4 alkylthio, C2-C5 acyloxy or C1-C4 alkyl, and wherein R2 represents hydrogen or C1-C4 alkyl, and wherein n is an integer from 1 to 12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein Xi independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and with the proviso that at least one of the Xi is not CH2, and with the proviso that if R1 is an alkye, then the carbon-carbon triple bond is positioned between the (ω-1) carbon and the (ω-2) carbon, or between the (ω-2) carbon and the (ω-3) carbon, or between the (ω-3) carbon and the (ω-4) carbon, a salt, prodrug or complex thereof, which can be used for the treatment and/or prevention of syndrome X, obesity, hypertension, fatty liver, diabetes, hyperglycaemia, hyperinsulinemia and stenosis. Further, the invention relates to a nutritional composition comprising said fatty acid analogues, and a method for reducing the total weight, or the amount of adipose tissue in an animal.
WO2010082531A1 Active blood coagulation factor inhibitor Provided are a novel salt form of a compound, which exhibits a function to inhibit the active blood coagulation factor X and is thus useful as a medicine for preventing/treating thrombotic diseases, and a crystal thereof. Provided are a salt of a tartaric acid and a crystal thereof as a novel salt form of an N1-(5-chloropyridine-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-yl)carbonyl]amino}cyclohexyl)ethanediamide and a crystal thereof.
US7550507 2-(alpha-hydroxypentyl) benzoate and its preparation and use The invention relates to new synthetic 2-(α-hydroxypentyl) benzoates, their preparation and pharmaceutical compositions containing such salts as active ingredients. The invention also relates to the use of the compounds for preventing and treating cardioischemia, cerebroischemia and cardiac or cerebral arterial occlusion (obstruction), etc.
CN103483363A Diverse chiral amino boric acid, preparation method and application thereof The present invention discloses a diverse chiral amino boric acid, a preparation method and an application thereof, wherein the diverse chiral amino boric acid is a compound represented by a formula (I) or a formula (II). The diverse chiral amino boric acid has the following characteristics that: the library containing rich compounds with the type is provided for researches on new drugs, a yield and stereoselectivity can be increased, the preparation cost of the class 2 drugs can be reduced, the synthesis route of the class 2 drugs can be simplified, and good economic benefits are provided.
EP2358689A1 Benzothiazole derivatives as anticancer agents Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula (I) wherein each symbol is as defined in the present specification, or a salt thereof.
US20050014835 Agents for Treating Diseases Caused by Nonsense Mutations The present invention comprises compositions for treating diseases caused by nonsense mutations, including dipeptide antibiotics of Formula (I) shown below, such as negamycin. Unlike aminoglycoside antibiotics such as gentamicin, dipeptide antibiotics can induce the expression of mature proteins by readthrough nonsense mutations without generating serious side effects.
EP1523335A2 Injectable depot formulation comprising crystals of iloperidone An injectable depot formulation comprising crystals having Structure (I) wherein R is (FII) and the X5o value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolite have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.
WO2006073366A1 Non-anilinic derivatives of isothiazol-3(2h)-one 1,1-dioxides as liver x receptor modulators The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
CN101032477A Electrolyte complementary medical combination for injection The electrolyte replenishing medicine composition for injection contains potassium aspartate and magnesium aspartate in the weight ratio of 1 to 1 as effective components, mannitol as freeze drying excipient and pH regulator, with the ratio between total weight of potassium aspartate and magnesium aspartate and the weight of mannitol being 10 to 7.
WO2012153313A1 Pharmaceutical composition of febuxostat The present invention relates to an immediate-release febuxostat composition and process of preparation for the same. It also relates to a method of treating gout and hyperuricemia using the composition of the present invention.
WO2010023474A1 Novel polymorphs of sunitinib and processes for their preparation The present invention relates to novel polymorphs of sunitinib free base designated form II and form III and to processes for their preparation. The invention also relates to their use as APIs and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising said novel polymorphs and salts, solvates and hydrates prepared according to the invention,and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.
US8350060 2-amino-bicyclo[3.1.0] hexane-2, 6-dicarboxylic ester derivative A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.
US20100311715 Alpha carbolines and uses thereof This invention provides alpha-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, and x are as described in the specification. The compounds are useful for treating inflammatory diseases and cancer.
WO2007062468A1 Biologically active compounds Compounds having useful biological activity, particularly antioxidant and anti-inflammatory activity, derived from Centipeda cunninghamii, and biologically active derivatives thereof, pharmaceutical compositions comprising these compounds, and prophylactic and therapeutic use of the compounds.
CN102499945A New application of bacterial endotoxin The invention discloses a new application of bacterial endotoxin, namely application of bacterial endotoxin in preparation of a medicament for treating and preventing allergic constitution diseases. Bacterial endotoxin in intestinal tract is translocated to enter into blood circulation so as to induce intestine-derived endotoxemia, which is an important internal cause of aging of a human body and allergic disease and cancer. After an edible bacterial endotoxin preparation is taken orally, the trans location of the intestinal tract endotoxin is effectively inhibited, an immunization and irritation adjusting effect is achieved, and when the human body contacts bacterial endotoxin frequently and is administered with high-dose bacterial endotoxin, the human body only appears slight response or no response (hyporesponsiveness), so as to build immunization tolerance for deallergization. The bacterial endotoxin is used for preventing and treating I, II, III and IV type hypersensitive diseases such as eczema, urticaria, allelgic asthma, diabetes mellitus, hyperthyroidism, uremia, lupus erythematosus, psoriasis, various ulcers and burn and scald, preventing aging and resisting cancers.
US20100168132 Quinuclidine derivatives and their use as muscarinic m3 receptor antagonists Compounds of Formula (I) ; in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
US20100074973 Thioxanthene modulators of dopamine d2 receptors The present invention relates to new thioxanthene modulators of dopamine D2 receptors, pharmaceutical compositions thereof, and methods of use thereof.
CN102974025A Disposable cervical dilator attached with medicine film The invention provides a disposable cervical dilator attached with a medicine film, and a preparation method of the disposable cervical dilator with the medicine film. The cervical dilator is attached with the medicine film of local anesthetics; when the disposable cervical dilator is used, the medicine film is swollen and dissolved under body temperature; and medicines in the medicine film are released out, and are absorbed by a cervical mucous membrane, so that pain of patients is relieved, and occurrences of adverse reactions are reduced. The disposable cervical dilator with the medicine film is convenient to use, and simple and feasible in preparation process; the related pharmaceutic adjuvants are all easy to purchase and are low in cost; and the disposable cervical dilator has good social and economic benefits.
CN103349661A Preparation method and application of formononetin-5-FU mixture The invention discloses a medicine (formononetin-5-FU (5-fluorouracil) mixture) for curing colorectal cancer drug resistance and a preparation method thereof. The method comprises the followings: adding fetal calf serum, penicillin and streptomycin into the RPM1-1640 culture medium, subpackaging through centrifuge tubes after sufficient mixing, and reserving at the temperature of 4 DEG C for standby application, namely complete culture solution is obtained; under photophobic condition, weighing 5-fluorouracil powder by using an electronic balance, adding the complete culture solution, and after complete resolution, obtaining 5-fluorouracil mother liquor through preparing; then sterilizing through a millipore filter, namely obtaining liquid A; weighing formononetin powder by using the electronic balance, adopting dimethyl sulfoxide for hydrotropy until complete resolution, and preparing the formononetin mother liquor; subpackaging and diluting so as to enable the final concentration of dimethyl sulfoxide to be lower than 1 per thousand and then to be 50 umol/L through multiple proportion dilution, namely obtaining liquid B; mixing the liquid A and the liquid B through vibration of a vibration machine, namely obtaining the formononetin-5-FU mixture. The formononetin-5-FU mixture provided by the invention is used for treating colorectal cancer drug resistance, the effect is obvious, the raw material cost is low, and the preparation method is simple.
US7476743 Treating cellular proliferation disease with 1,2,5-triazol-5-one and as an anticancer agent and inhibitor of kinesins for treatment of hyperplasia or restenosis 1,2,4-Tiazole-5-ones useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
CN1938274A Novel piperidines as chemokine modulators (CCR) Compounds of Formula (I) are modulators of chemokine (for example CCR3) activity (for use in, for example, treating asthma).
US20090215691 NOGO Receptor Antagonists Disclosed are immunogenic Nogo receptor-1 polypeptides, Nogo receptor-1 antibodies, antigen-binding fragments thereof, soluble Nogo receptors and fusion proteins thereof and nucleic acids encoding the same. Also disclosed are compositions comprising, and methods for making and using, such Nogo receptor antibodies, antigen-binding fragments thereof, soluble Nogo receptors and fusion proteins thereof and nucleic acids encoding the same.
WO2013092509A1 Inhibitors of sialoadhesin for the treatment of diseases caused by enveloped viruses The present invention refers to methods and compositions to prevent viral entry into cells expressing the CD169/sialoadhesin surface receptor by inhibiting the coupling of the sialyllactose molecule contained in the viral membrane gangliosides to the CD 169/ sialoadhesin receptor. The invention also pertains to vaccine compositions based on dendritic cells loaded with an antigen of interest whereby the vaccine is provided together with a composition capable of preventing viral entry into cells expressing the CD169/sialoadhesin. Moreover, the invention relates to diagnostic and therapeutic compositions that can be specifically delivered to enveloped virions wherein the diagnostic/therapeutic agent is coupled to CD169/sialoadhesin.
WO2013178575A1 New indanyloxyphenylcyclopropanecarb oxylic acids The present invention relates to compounds of general formula I, (I) wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
US7732487 Administering calcium channel modulators such as 13,14-dihydro 15-keto-16,16-difluoroprostaglandin E1, for prophylaxis of brain, cardiovascular, gastrointerstinal, respiratory system, vision or liver disorders Disclosed is a method for prophylactic or therapeutic treatment of a condition or disease responsive to opening of ClC-2 channel, which comprises the step of administrating an effective amount of a ClC-2 channel opener to a subject in need of said treatment. According to the invention, a tissue or organ to be transplanted can also be treated with the ClC-2 channel opener.
CN103656047A Lemai pill composition with high paeoniflorin content The invention discloses a Lemai pill composition with high paeoniflorin content. The Lemai pill composition is prepared by the following method: weighing the following components by weight according to a formula: 79.84 parts of salvia miltiorrhiza, 39.92 parts of ligusticum wallichii, 39.92 parts of red paeony root, 39.92 parts of red flower, 19.96 parts of rhizoma cyperi, 19.96 parts of elecampane and 9.98 parts of hawthorn; adding 249.504 kg of the previous seven medicinal materials into an extracting tank, adding water for decocting for several times, collecting the filtrate each time and merging the filtrate, merging the filtrate and concentrating to obtain extract with the relative density of 1.1-1.3; performing alcohol precipitation on the extract by using ethanol, wherein the addition amount of the ethanol is 30-70 weight percent of the mass of the extract, and the alcohol precipitation time is 18-24 hours; recovering the ethanol after alcohol precipitation, and preparing pills according to a conventional pill preparation process, the paeoniflorin content in the Lemai pill composition is more than or equal to 1.0 percent finally. According to the Lemai pill composition prepared in the invention, the content of a target component, namely the paeoniflorin, is greatly improved, and the Lemai pill composition is suitable for industrial large-scale production.
WO2007041053A3 Formulation comprising metformin and vildagli ptin This invention relates to a formulation comprising a dipeptidylpeptidase IV (DPP-IV) inhibitor preferably vildagliptin and metformin, to tablets comprising such formulations and to processes for the preparation thereof.
CN101049286B Gel preparation of Ciclopirox Olamine A gel medicine containing ciclopirox olamine for skin and vagina is proportionally prepared from ciclopirox olamine, carbomer, alcohol, propanediol, triethanolamine, bisodium versenate, polysorbide, and water. Its preparing process is also disclosed.
CN103083242A Preparation method of carboxymethyl chitosan nanoparticle Belonging to the technical field of veterinary drugs, the invention discloses a preparation method of a carboxymethyl chitosan nanoparticle. According to the method, ceftiofur is taken as a main component, carboxymethyl chitosan is adopted as a carrier, and the ceftiofur and the carboxymethyl chitosan are in a weight ratio of 1:10-1:30, optimally a weight of 1:4-1:8. The prepared carboxymethyl chitosan nanoparticle is round and regular in shape and free of aggregation phenomenon, and has a small particle size and narrow particle size distribution. Animal experiments with rabbits as the animal model show that compared with traditional ceftiofur preparations, carboxymethyl chitosan embedded ceftiofur has the characteristics of faster absorption and higher bioavailability.
EP1320357B1 Topical polymeric antimicrobial emulsion An emulsion composition for the topical application comprising: (a) A polymeric oily phase; (b) A polymeric emulsifier; (c) An aqueous phase; (d) A polymeric antimicrobial andoptionally one or more components selected from polymeric film formers, inorganic and polymeric stabilizers, other inorganic or polymeric excipients and mixtures thereof.
CN103655546A Application of jaceosidin in preparation of drugs used for preventing or treating pulmonary fibrosis The invention provides novel pharmaceutical purposes of jaceosidin and specifically relates to application of jaceosidin in prevention or treatment of pulmonary fibrosis, wherein through inhibition of pulmonary epithelial-mesenchymal transition, pulmonary vascular endothelial-mesenchymal transition and propagation of fibroblasts, growth and development of pulmonary fibrosis are inhibited, so prevention or treatment of pulmonary fibrosis is realized. In the above-mentioned application, the dosage range of applied jaceosidin is 20 to 1000 mg, preferably, 20 to 500 mg.
WO2007123939A8 Novel arylamino n-heteraryls as mek inhibitors The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed. is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
US20110060015 5-[5-[2-(3,5-BIS(Trifluoromethyl)Phenyl)-2-MethylpropanoMethylpropanoylmethylamino]-4-(4-Fluoro-2-Methylphenyl)]-2-Pyridinyl-2-Alkyl-Prolinamide As NK1 Receptor Antagonists The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.
US20050176787 Thiazolidinediones alone or in combination with other therapeutic agents for inhibiting or reducing tumour growth Use of thiazolidinedione derivatives for the preparation of medicaments for inhibiting or reducing tumour growth or metastases, alone or in combination with an RXR agonist or well-known antitumour agent.
WO2009151691A2 Genetic polymorphisms associated wiith venous thrombosis, methods of detection and uses thereof The present invention is based on the discovery of genetic polymorphisms that are associated with venous thrombosis. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.
US20050049424 6-Hydroxy isoflavones derivatives and medicaments involving same Isoflavone compounds of the formula (I) or (II) Where R can be R 7? or OR 7? or O and the formula (III) is either a single or double bond extends to Y then Y is an optionally substituted benzyl. W, R 1?, Z o? R 2? and R 7? are as defined in the specification. The compounds are useful for the treatment of certain diseases and disorders, including cancer and inflammation.
US20060099691 Production of complex carbohydrates Compositions and methods for making complex carbohydrates in a bacterial production cell are disclosed. The complex carbohydrates that can be made include oligosaccharides and polysaccharides of bacterial or mammalian origin.
US20120202798 COMPOSITIONS CONTROLLING pH RANGE OF RELEASE AND/OR RELEASE RATE The present invention provides a composition controlling a pH range of release and/or a release rate, which contains (i) a thienotriazolodiazepine compound of the formula (I) and (ii) at least one kind of ingredient selected from the group consisting of a water-soluble polymer, an enteric polymer, a water-insoluble polymer and a porous polymer and/or a surfactant, as well as a production method thereof.
US8278329 Antagonizing N-type calcium channels; use as analgesic, neurodegenerative diseases, brain injury, bronchial asthma, unstable angina and irritable colitis, drug withdrawal symptoms; t-butyl 2-[4-(5H-dibenzo[a,d][7]annulen-5-ylidene)-1-piperidinyl]-2-oxoethylcarbamate for example The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating pain etc. comprising the compound represented by the following general formula (1) or its analogue to a patient in need of such treatment: wherein, A represents CH═CH, etc., a, b, c and d represents CH etc., R1, R2, R3, R4, R5 and R6 represents H etc., V—W represents C═C, etc., n represents 0 to 3, Y1 represents O etc., B represents —(CH2)vCHR21 wherein v is 0 to 3, R21 represents H, a lower alkyl group or the like, etc., G represents —CO—, a covalent bond, etc., m is 0 to 6, R7 and R8 represents H, a lower alkyl group, —COR18a, —COOR20 wherein R18a and R20 each represents a lower alkyl group or the like, etc.
CN101856383A Liver-protecting white spirit and preparation method thereof The invention discloses liver-protecting white spirit and a preparation method thereof. The technical problem needing to be solved is to protect the liver of a human body when people drink white spirit. The liver-protecting white spirit has white spirit, wherein each 500ml of white spirit contains 10-2000mg of resveratrol, 5-1000mg of ganoderma lucidum extract and 5-1000mg of rhodiola root extract. The preparation method of the liver-protecting white spirit is obtained by adopting the following steps of: adding 10-2000mg of resveratrol, 5-1000mg of ganoderma lucidum extract and 5-1000mg of rhodiola root extract into 500ml of white spirit of 30-60 degrees and stirring evenly so as to obtain the liver-protecting white spirit. Compared with the prior art, the invention exerts the liver-protecting and fat-lowering functions of veratryl alcohol, the ganoderma lucidum extract and the rhodiola root extract and also keeps the original characteristics of the white spirit by dissolving the effective components of the natural plants of grape, ganoderma lucidum and rhodiola root into the white spirit .
US20100055158 Environmentally Activated Compositions, Articles and Methods An article includes a film layer; at least one layer of adhesive on at least one side of the film layer; a patch or strip comprising at least one antimicrobial agent, the patch or strip disposed on the same side of the film layer as the at least one layer of adhesive; and a relatively non-flexible sheet releasably attached to the side of the film layer opposite to the patch or strip. Alternatively, an article includes a film layer; a collagen layer; and a biodegradable hydrogel layer comprising PHMB; wherein the biodegradable hydrogel layer comprising PHMB is disposed between the film layer and the collagen layer
CN1636978A Pyrrolidinyl metalloprotease inhibitor and its application The present invention is pyrrolidinyl matrix metalloprotease inhibitor and its application. One kind of powerful matrix metalloprotease inhibitor is provided to treat disease with abnormal matrix metalloprotease activity expression effectively. Specifically, the present invention relates to the compound, various optical isomers, pharmaceutically acceptable salts, solution and precursor medicine. The present invention also relates to their pharmaceutical use.
WO2010149653A1 A pharmaceutical composition comprising meldonium succinate and medical uses thereof A pharmaceutical composition with cardioprotective, antiischemic, antihypoxic and antioxidant properties for prevention and/or treatment of disorders, selected from the group of dyslipidemia, hyperlipidemia, atherosclerosis, coronary heart disease as chosen from the group of angina pectoris and myocardial infarction, chronic heart failure, transient and permanent ischemic attack including cerebrovascular accident and stroke and peripheral arterial occlusive disease, comprising Meldonium succinate alone or in the combination with inorganic succinate.
CN1742709A Method for extracting high-content solanesol extract by liquid-liquid two-phase method The method for extracting high-content solanesol by utilizing liquid-liquid two-phase extraction process is characterized by that said method includes the following steps: adding 800-2000 weight portions of broken tobacco segments into a four-mouth flask with stirrer, thermometer and reflux condenser, respectively adding 600-2800 weight portions of polar solvent, 600-2800 weight portions of non-polar solvent and 1-10 weight portions of stabilizing agent, reflux extracting for 2-4hr at 40-100deg.C and taking out extract; then using identical method to make secondary extraction, combining two extracts, cooling, filtering, standing still to make phase separation to respectively obtain 100-5600 weight portions of non-polar solution and 1200-5600 weight portions of polar solution, respectively recovering solvent to obtain 20-100 weight portions of extract in which the brownish yellow solanesol content is 17-24% and 30-120 weight portions of alcoholic extract containing no solanesol.
US20080249116 Aldehyde dehydrogenase; 3-(4-hydroxyphenyl)-7-[(5-phenyl(1,2,4-oxadiazol-3-yl))methoxy]-3-hydroquinazolin-4-one; alcoholism; cocaine and nicotine addictions Disclosed are novel quinazolinone derivatives, useful as ALDH-2 inhibitors for treating mammals for various disease states, such as treatment for cocaine dependency or alcohol dependency.
CN102372679A Febuxostat water-soluble derivative and preparation method thereof The invention provides a febuxostat water-soluble derivative expressed by a general formula I, wherein M represents choline, lysine, arginine, diethylamine, triethylamine, diethanol amine and triethanolamine. The lysine or arginine can be selected from an L configuration, a D configuration or a DL configuration.
EP0952851B1 Anti-carious chewing gums, candies, gels, toothpastes and dentifrices The invention relates to anticarious delivery vehicles, specifically chewing-gums, candies, confectioneries, toothpastes, dentifrices and gels. The invention specifically provides chewing gums, candies, confectioneries, toothpastes, dentifrices and gels containing non-toxic sparingly soluble calcium and phosphate compounds as additives, causing the release of calcium and phosphate ions into the oral cavity gradually and persistently for a period no less than 5 minutes. The invention provides released calcium phosphate ions that diffuse into partially demineralized tooth enamel or dentin, leading to remineralization and repair of caries lesions, dental plaque, open dentinal tubules and exposed dentin. The invention thus provides agents and methods for remineralization of teeth and for reducing or eradicating cariogenic challenge in plaque following sucrose intake. The formulations of the invention can thereby produce effective anticaries actions without the use of fluoride. In addition, the formulations of the invention can be used to desensitize hypersensitive teeth.
EP2446884A1 Composition for inhibiting inflammation comprising hyaluronic acid and a hmg-coa reductase inhibitor A pharmaceutical composition for inhibiting inflammation, comprising (a) hyaluronic acid, (b) a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, and (c) a pharmaceutically acceptable carrier, is provided. Also provided is a method for inhibiting inflammation in a mammal, comprising administrating to the mammal an effective amount of a composition comprising (a) hyaluronic acid and (b) an HMG-CoA reductase inhibitor.
CN103416537A Selenium-rich blood nourishing tea and production method thereof The invention relates to a selenium-rich blood nourishing tea and a production method thereof. The selenium-rich blood nourishing tea is characterized by comprising the following materials in percentage by weight: 15 to 20 percent of selenium-rich angelica sinensis leaves, 10 to 20 percent of medlar, 10 to 20 percent of selenium-rich astragalus extract, 5 to 10 percent of carthamus tinctorius, 5 to 15 percent of persimmon leaves, and 30 to 45 percent of selenium-rich black tea. The production method comprises the following steps in sequence: uniformly mixing the powder of the four ingredients (the selenium-rich angelica sinensis leaves, the medlar, the persimmon leaves and the black tea) and selenium-rich astragalus extract according to dosages; bagging; sealing; sterilizing; packaging to obtain the selenium-rich blood nourishing tea. The selenium-rich blood nourishing tea is a nutrient health-protection drinking mainly blended for anemia patients, women in menstrual period to regulate vital energy and blood, and women suffering from dysmenorrheal and irregular menstruation.
US20100234366 Use of Strobilurins for the Treatment of Disorders of Iron Metabolism Strobilurin derivatives can be employed for the treatment and/or prevention of disorders of iron metabolism in mammals.
WO2008086462A3 AMINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS INHIBITORS OF β-CANTENIN/TCF-4 PATHWAY AND CANCER TREATMENT AGENTS The present invention relates to amino-substituted quinazoline derivatives as inhibitors of β-catenin/tcf-4 pathway, which can be useful in the treatment of cancer; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.
US20120059022 Crystalline Form of Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoicacid] Calcium Salt Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.
CN102973511A Amoxicillin dry suspension and preparation method thereof The invention belongs to the field of veterinary medicine preparations and particularly relates to an amoxicillin dry suspension and a preparation method thereof. The dry suspension is composed of by weight: 2.5-15% of amoxicillin, 15.0-30.0% of a suspending agent, and 55.0-82.5% of an auxiliary material. The amoxicillin dry suspension of the present invention is convenient for administration, good in uniformity and high in bioavailability.
US20120238566 Use of cell autophagy (type ii cell apoptosis) inhibitors Use of cell autophagy (type II cell apoptosis) inhibitors for preventing and/or treating avian influenza, injury of lungs caused by avian influenza virus or nanometer materials. The cell autophagy (type II cell apoptosis) inhibitors are selected from 3-methyladenine, SB203580, LY294002, and or wortmannin. The injury of lungs includes acute respiratory distress syndrome. The avian influenza virus is H5N1, H5N2 or H9N2 avian influenza virus. The nanometer materials include PAMAM G3, G4, G5, G5.5, G6, G7, or G8.
EP1268441B1 An intermediate and process for its synthesis The invention relates to the compound of formula (I) and to a process for procuding the compound of formula (I).
WO2014110189A1 Deuterated momelotinib The present invention in one embodiment provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification.
EP2349290A1 Use of helium-oxygen gas mixtures for treating pulmonary arterial hypertension The present application relates to the use of helium-oxygen gas mixtures for treating and/or preventing primary and secondary forms of pulmonary hypertension (PH) and to the combination of pharmaceutical drugs with helium-oxygen gas mixtures, wherein the gas mixtures serve as carrier gases for improving the incorporation of a drug for treating and/or preventing pulmonary hypertension.
US20100317671 Xanthine-based cyclic gmp-enhancing rho-kinase inhibitor inhibits physiological activities of lung epithelial cell line A pharmaceutical composition for a treatment of an interstitial lung disease is provided. The pharmaceutical composition comprises an effective amount of an active component being one selected from a group consisting of a KMUP compound, a KMUP monoquaternary ammonium salt and a KMUP monoquaternary ammonium complex salt, wherein the KMUP monoquaternary ammonium complex salt is synthesized by the KMUP compound and a carboxylic acid derivative of one selected from a group consisting of a statin, a non-steroid anti-inflammatory (NSAIDs) and an anti-asthmatic drug.
US20060233807 Novel therapies and methods of screening for therapeutic compounds A method for killing cells, said method comprising introducing into the nucleus of the cell, a moiety (other than HAMLET) which inhibits histone activity. This method will be useful for example in the treatment of cancer for antibacterial activity. Histones can be used as a basis of screening methods to select therapeutic compounds, and these are also described and claimed.
US20090170949 Method To Control Body Weight The present invention relates to a method to treat obesity and/or a method to lose or control body weight. More specifically, the invention relates to the use of a compound inhibiting the sweet taste perception, preferably by inactivating the T1R3 receptor, for the preparation of a medicament to treat or prevent obesity and/or to treat or prevent diabetes and/or to lose or control body weight.
CN102920699A Application of 2-phenylimino-5-(4-dimethylamino benzylidene)-4-thiazolidone to preparation of anti-breast cancer medicament The invention discloses an application of 2-phenylimino-5-(4-dimethylamino benzylidene)-4-thiazolidone to preparation of an anti-breast cancer medicament. The compound can be used for causing 50 percent of the growth inhibiting effect of MDA-MB-231 breast cancer cells at the amount of 0.4muM, causing cell cycle arrest and inducing apoptosis of breast cancer cells at the amount of 2.0muM, has the effect of effectively inhibiting the growth of mouse solid tumors and is free from remarkable toxic and side effects. The compound disclosed by the invention is expected to become an effective anticancer medicament for treating triple negative breast cancer for which the quantity of selectable medicaments is small, and has good development and application prospects.
CN101406649B Total alkaloid extract, and extraction method thereof and use in preparing medicament for treating cough The invention belongs to the field of pharmaceutical chemistry and discloses an effective total alkaloid extract of stemonaceae stemona sessilifolia, an extraction method thereof and application in preparing a medicine for treating cough. The effective total alkaloid extract of stemonaceae stemona sessilifolia has the activity of relieving and/or inhibiting cough.
US20100008982 Non-covalent complexes of bioactive agents with starch for oral delivery The present invention relates to particles comprising non-covalent complexes which comprise starch and an active agent and dry compositions containing such particles for the oral delivery of the active agents. Preferably the particles are degraded and release the active agent within the intestines, protecting the active agent from degradation in the stomach. The present invention further relates to methods for preparing suspensions of these particles having a uniform particle size in the range of several microns.
CN103145569A Crystal form B of dapoxetine hydrochloride, and preparation method thereof The invention relates to a crystal form B of dapoxetine hydrochloride which is a drug for treating male premature ejaculation, and a preparation method thereof. The crystal form B of dapoxetine hydrochloride is characterized in that the X-ray powder diffraction pattern thereof has corresponding characteristic diffraction peaks at positions of 2[theta] angle values being 9.2 degrees, 14.7 degrees, 16.2 degrees, 16.9 degrees, 18.0 degrees, 21.8 degrees, 23.2 degrees, 24.9 degrees, and 27.1 degrees.
US20100215620 The co-culture method of sphingomonas sp. bacterial strain and aspergillus sp. fungus strain, new anti-cancer and antibiotic glionitrins derived from this co-culture method, and pharmaceutical composition containing glionitrins or pharmaceutically acceptable salt thereof as an active ingredient The present invention relates to a co-culture method of Sphingomonas sp. bacterial strain and Aspergillus sp. fungus strain, in which the novel Sphingomonas sp. bacterial strain KMK-001 is cultured in a liquid medium and the novel Aspergillus sp. strain KMC-901 separately cultured in another liquid medium is added to the above culture solution, a novel glionitrin biosynthesized therefrom and a pharmaceutical composition comprising the said glionitrin or its pharmaceutically acceptable salt as an active ingredient. The glionitrin herein has strong cytotoxic effect on cancer cells and has antibiotic effect on 10 pathogenic bacteria including the novel Sphingomonas sp. bacterial strain KMK-001, so that it can be effectively applied in antibiotics or anti-cancer agents.
CN102791264A Oil and fat composition for prevention or treatment of diabetes Provided is an oil and fat composition that is highly safe and is effective for the prevention or treatment of diabetes without concern over side effects, even when ingested on a continuous basis. The oil and fat composition for the prevention or treatment of diabetes comprises triacylglycerol as an active ingredient, and this triacylglycerol has one or two medium-chain fatty acid residues per molecule and comprises as the structural fatty acids a C6-10 medium-chain fatty acid and a C16-24 long-chain fatty acid.
CN102988679A Medicinal composition for tonifying kidney and spleen and preventing and treating osteoporosis The invention provides a medicinal composition for tonifying kidney and spleen and preventing and treating osteoporosis. The medicinal composition is characterized by comprising the following components in parts by weight: 30 to 60 parts of chondroitin sulfate, 8 to 15 parts of astragalus, 8 to 12 parts of codonopsis pilosula, 8 to 12 parts of fried bighead atractylodes rhizome, and 8 to 12 parts of fried yam. The product has good effect of preventing and treating osteoporosis.
US20100305149 Polyal Drug Conjugates Comprising Variable Rate-Releasing Linkers Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described.
CN101037435A (S)-nifuratel, preparation method and application thereof The invention discloses a nifuratel with a optical activity. Specifically, the invention provides a (S)-nifuratel, i.e. (S)-5-[(methylthio)methyl]-3-[(5-nitryl-2-furan)methylene]amido]-2-oxazolidone, the producing method and the combination including the optical activity compound. Compared to the racemic nifuratel, (S)-nifuratel has a better anti-inflammatory and anti-fungi activity. The invention also discloses the producing method for (S)-nifuratel which has the (S)-chloroepoxy propane as initial material, adopts the 3-dimension and selective synthesis method and produce a high optical purity (S)-nifuratel with a high yield.
CN103099794A Vitamin C clathrate dispersible tablet The invention relates to a vitamin C clathrate dispersible tablet. Firstly, vitamin C is prepared into a clathrate, which is then prepared into a dispersible tablet.
DE102007010077A1 Use of 1,3-dioxane derivatives to enhance the activity of gamma-aminobutyric acid (GABA) on GABA-A receptors 1,3-Dioxane derivatives (I) are used to enhance the activity of gamma-aminobutyric acid (GABA) on GABA-A receptors. 1,3-Dioxane derivatives of formula (I) are used to enhance the activity of gamma-aminobutyric acid (GABA) on GABA-A receptors. R 1-R 3H, 1-6C haloalkyl, 1-6C alkyl or 1-6C alkoxy; R 4-R 6H, 1-3C alkyl or 1-3C haloalkyl; R 7H or 1-3C alkyl; R 1+R 7= a bridge stated to be of formula C(R 4) n; n : 1-3. Independent claims are also included for: (1) 2-R 5-4-R 4-4-Ar 1-6-R 6-1,3-dioxanes (Ia), 2,5,6-trimethyl-4-Ar 2-1,3-dioxanes, 2,6-dimethyl-4-Ar 3-1,3-dioxanes and 4-methyl-4-Ar 4-1,3-dioxanes; (2) a process for preparing (Ia). Ar 1phenyl optionally monosubstituted with Me, Et, Pr, Bu, halo or trihalomethyl; R 4-R 6= Me or trihalomethyl, but not all Me when Ar 1= unsubstituted phenyl; Ar 2phenyl optionally monosubstituted with Me, Et, Pr or Bu; Ar 3phenyl monosubstituted with Et, Pr or Bu; Ar 4phenyl monosubstituted with Me, Et, Pr or Bu. [Image] - ACTIVITY : Antidepressant; Tranquilizer; Anticonvulsant; Neuroprotective; Nootropic; Antimigraine. Mice injected with 2,4,6-trimethyl-4-(4-meth ylphenyl)-1,3-dioxane (0.5 g/kg) were observed for movement activity over 30 minutes. The mean travel distance was reduced by 87% compared with control mice. - MECHANISM OF ACTION : gamma-aminobutyric acid (GABA) receptor activator.
CN1857270A Penciclovir gel and its preparing method The present invention provides a kind of new penciclovir preparation form, penciclovir gel. The penciclovir gel consists of penciclovir, matrix, pH regulator and water. The preparation process of the penciclovir gel includes dissolving penciclovir and pH regulator in water through heating and stirring to obtain penciclovir solution; mixing with the hydrophilic matrix; adding pure water to required amount; and vacuumizing to eliminate bubble, filling and sealing to obtain penciclovir gel product. Compared with available cream, the penciclovir gel is comfortable and has no greasy feeling.
US20100190768 Novel fused pyrole derivative The present invention relates to a compound represented by the formula (1) which is useful as a glucocorticoid receptor function regulating agent, an anti-inflammatory agent or an antidiabetic agent, or a pharmaceutically acceptable salt thereof: wherein R1 is aralkyl, etc.; R2 is H, etc.; —W4═W5—W6═W7— is a group of the formula: —CR4═CR5—CR6═CR7— (in which R4, R5, R6 and R7 are independently a group of the formula: -E-A (E is a single bond, etc., A is H or nitro, etc.)), etc.; R8 is a group of the formula: —OR11 (R11 is H, etc.), etc.; R9 is trifluoromethyl, etc.; R10 is a group of the formula: —[C(R13)(R14)]n—R15 (R13 and R14 are independently H, etc., n is an integer of 0 to 10, R15 is a group of the formula: N(R18)R19 (R18 and R19 form a nitrogen-containing heteromonocycle together with a nitrogen atom to which they are bonded), etc.).
WO2005011734A3 Composition of a vegf antagonist and an anti-proliferative agent and its use for the treatment of cancer Methods of treating cancer and/or reducing or inhibiting tumor growth in a subject in need thereof, comprising administering pharmaceutical composition comprising a vascular endothelial cell growth factor (VEGF) antagonist, such as a VEGF trap, an anti-proliferative agent, such as taxol, and a pharmaceutically acceptable carrier.
CN102743328A Intrauterine sustained control release drug delivery system adopting biodegradation material, and preparation method thereof The present invention relates to a female intrauterine drug delivery system, and more particularly to an intrauterine sustained control release drug delivery system adopting a biodegradation material, and a preparation method thereof. The present invention provides an intrauterine sustained control release drug delivery system adopting a biodegradation material, and a preparation method thereof, wherein the system has characteristics of short length, light weight, efficiency, and reversibility. The system comprises a sustained control release pipe, a drug core and a tail filament, wherein the sustained control release pipe is wrapped on the external of the drug core, the tail filament is positioned between the sustained control release pipe and the drug core or is accommodated in the middle of the drug core, the drug core is a rod prepared by blending progesterone or an available intrauterine sustained control release drug and a biodegradable polymer, and the sustained control release pipe is made of a biodegradable polymer. The system of the present invention has characteristics of no stent, no copper ion, safety, practicality, and simple placement technology.
WO2009100375A1 Substituted imidazopyridazines useful as kinase inhibitors The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.
WO2007069716A1 Composition having effect of inhibiting visceral fat accumulation A composition which contains a component prepared by defatting fish proteins, fish peptides and/or fish amino acids while remaining fish proteins as such or digesting the same by a protease. As the fish proteins employed as the starting material, fish proteins of white fishes, in particular, cod fishes are preferred. This composition exerts an effect of inhibiting the accumulation of visceral fat that requires extra attention among risk factors for obesity, has a high safety and can be taken as a food.
US20120289561 Combinations of fesoterodine and salivary stimulants for the treatment of overactive bladder Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release fesoterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release fesoterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of alleviating a side effect of treatment for overactive bladder in a patient suffering therefrom, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release fesoterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.
WO2008071870A3 Use of agomelatine in order to obtain drugs intended for the treatment of smith-magenis syndrome The invention relates to the use of agomelatine or N-[2-(7-methoxy-1-naphtyl)ethyl]acetamide in order to obtain drugs intended for the treatment of Smith-Magenis syndrome.
WO2012078492A1 A combination therapy with lenalidomide and a cdk inhibitor for treating multiple myeloma Provided herein are methods for the treatment of multiple myeloma, wherein the methods comprise administration of lenalidomide and administration of a CDK inhibitor.
CN102824637A Application of TRPC5 as drug target in reversing multi-drug resistance The invention provides a novel purpose of TRPC5, which is an application of TRPC5 as drug target in reversing multi-drug resistance. The drug is an inhibitor for TRPC5, which comprises a pharmacology antagonist 2-APB of TRPC5, a blocking antibody T5E3 of TRPC5, a dominant inhibition plasmid pCDNA6-TRPC5-DN and Lenti-TRPC5-DN of TRPC5 and SiRNAsiC5 of TRPC5, and the multidrug resistance is generated by P-gp mediation. The invention has the key points that the TRPC5 is closely related to a P-gp protein expression of multidrug resistance generated by mediated tumor, and a TRPC5 inhibitor has obvious reversing effect on multidrug resistance of in vitro and in vivo tumor cells, accordingly, the application of TRPC5 as drug target in reversing multi-drug resistance provides the novel target for antineoplastic multidrug resistance medicine, and provides a novel clue for reversing the tumor multidrug resistance.
CN101716181B Invert sugar medicament composition liposome injection and new application thereof The invention discloses an invert sugar medicament composition liposome injection, comprising the following components in parts by weight: 1-20 parts of fructose, 1-20 parts of dextrose, 1-50 parts of yolk lecithin, 0.5-10 parts of poloxamer 188 and 1-30 parts of cholesterol.
EP1572685B1 Substituted benzodioxepins Disclosed are benzodioxepins of formula (I) and the physiologically acceptable salts and solvates thereof, R1, R2, R3, R4, A, B, a, and b having the meanings indicated in claim 1. Said benzodioxepins are ligands of the 5HT1A receptors and/or 5HT4 receptors while greatly inhibiting serotonin reuptake. The inventive benzodioxepins can be used for the treatment and prophylaxis of different diseases.
CN102343025A Aloe preparation and preparation method thereof The invention relates to an aloe preparation and a preparation method thereof, and the aloe preparation is characterized in that the preparation mainly comprises the following components by weight: 20-50% of aloe powder, 10-20% of vitamin E, and 39.5-59% of fructo oligosaccharides. The preparation method involves the selection of appropriate added auxiliary materials based on various dosage formsso as to prepare patent medicines which can be taken directly. The aloe preparation of the invention adopts aloe, vitamin E, and fructo oligosaccharides as main components, and can be directly prepared into Chinese patent medicines and health food with various dosage forms; with the synergistic effect of the three components, the aloe preparation effectively improves the internal environment of human intestines and stomach, promotes defecation, increases the generation of beneficial bacteria such as bifidobacteria and the like, promotes the absorption and utilization of nutrients in intestinal tracts, inhibits the generation of harmful bacteria such as escherichia coli and the like, reduces damage to human body caused by harmful toxins, and has the functions of beautification and gastrointestinal tract improvement; meanwhile the aloe preparation also inhibits the synthesis of tyrosinase active melanin, removes the generation of oxygen free radicals in cells, and has the functions of antioxidation, moistening, and cosmetic whitening.
US20050232952 Self emulsifying drug delivery systems for poorly soluble drugs A pharmaceutical composition in a form of a self-microemulsifying drug delivery system comprising: one or more therapeutic agent(s) which have low solubility in water or are water-insoluble, vitamin E, one co-solvent selected from propylene glycol and ethanol, one or more bile salts, TPGS, and one further surfactant selected from Tyloxapol and polyoxyl hydrogenated castor oil.
WO2014047221A1 Drug delivery systems and methods for treatment of bladder voiding dysfunction|and other lower urinary tract disorders by using trospium Methods, devices, and medicaments that include trospium are provided for use in the treatment of bladder dysfunction by locally administering the trospium into the bladder to achieve a sustained concentration of trospium in urine in the bladder sufficient to produce a therapeutic concentration of trospium in bladder tissue. The drug may be delivered into the bladder from an intravesical drug delivery device inserted into the bladder, wherein the device continuously releases the drug into the urine in the bladder over an extended period of hours or days.
US20090110737 Orally Disintegrating Powder Comprising Cilostazol and Mannitol The present invention provides an orally disintegrating powder comprising cilostazol as an active ingredient and mannitol in an amount of 70% by weight or more, which can be taken without water and can be disintegrated in oral cavity. Said powder is suitable for patients to whom cilostazol is applied, especially for aged patients and patients suffering from dysphagia.
WO2008103500A1 Thiazole derivatives as modulators of g protein-coupled receptors The invention provides compounds of formula (IA) or (IB) and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 120 (GPR120), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR120.
CN103536556A Pefloxacin mesylate composition freeze-dried powder for injection The invention provides a pefloxacin mesylate composition freeze-dried powder for injection, and belongs to the field of medicine and medicine preparation technology. The pefloxacin mesylate composition freeze-dried powder comprises following raw material ingredients, by weight, 7.26 to 9.17 parts of pefloxacin mesylate, 5.45 to 6.84 parts of chitosan nanoparticle, and 83.99 to 89.29 parts of injection water. Advantages of the pefloxacin mesylate composition freeze-dried powder are that: 1) the pefloxacin mesylate composition is capable of increasing antibacterial activities of pefloxacin mesylate on klebsiella, enterobacter and serratia significantly; 2) the size of the chitosan nanoparticle is ultra small, so that the chitosan nanoparticle is capable of passing through capillary vessels with a smallest diameter, and overcoming biological barriers, and rapid removing of the chitosan nanoparticle by macrophage is avoided, so that lasting time of the pefloxacin mesylate composition in blood is prolonged greatly; and 3) the chitosan nanoparticle can be used as a freeze-dried skeleton agent of the freeze-dried powder injection instead of mannitol so as to avoid active effects of mannitol on human bodies.
US20080014162 Method to treat skin in need of a calmative using at least one C-Glycoside derivative The present invention concerns a non-therapeutic method to prevent and/or treat a skin in need of a calmative using a C-glycoside derivative.
US20080280958 Administering a phosphodiesterase inhibitor; bioavailability; skin disorders; respiratory system disorders; using roflumilast A topical pharmaceutical preparation for administering a slightly soluble PDE4 inhibitor is described. A surprisingly good systemic bioavailability is observed with this dosage form.
CN102988278A Bromfenac sodium hydrate eye drops and preparation method thereof The invention discloses eye drops and a preparation method thereof, and particularly relates to bromfenac sodium hydrate eye drops and a preparation method thereof. The bromfenac sodium hydrate eye drops comprise the following constituents in percentage by weight: 0.1-0.2% of bromfenac sodium hydrate, 0.1-0.3% of Tween-80, 1-5% of povidone, 0.01-0.03% of edetate disodium, 0.2-0.5% of anhydrous sodium sulfite, 0.01-0.02% of benzalkonium bromide, 0.005-0.02% of boric acid, 0.005-0.02% of borax, 0.002-0.01% of sodium hydroxide, and the balance of water.
CN101518525A Preparation method for semi-pinnated brake herb extract injection The invention relates to a preparation method for a semi-pinnated brake herb extract injection. The preparation method comprises the following steps: directly mixing an active ingredient extract extracted from a plant semi-pinnated brake herb with an aqueous solution of basic hydroxides, basic salts or basic amino acids; stirring the mixture; keeping the pH value of 7.2 to 8.6; and adding an excipient to obtain the injection. The preparation process has moderate conditions; the extract compound molecules are ionized in the basic solution to obtain carboxylate anions; and therefore the method not only retains an anti-tumor activity structure, but also improves the solubility of the active ingredients. In addition, the basic matter is a micro-molecular compound, can enter a blood circulation system safely and is suitable for being prepared into water soluble injection. The injection has the characteristics of high solubility, good bioavailability, simple process, and low cost.
US20070249605 such as methyl 2-(4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetate This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.
US20100291091 Cancer associated gene ly6k LY6K is identified herein as a potential biomarker useful for the diagnosis of cancer, such as lung and esophageal cancers, as well as for the prognosis of patients with these diseases. As discussed in detail herein, LY6K is specifically over-expressed in most lung and esophageal cancer tissues examined, and is elevated in the sera of a large proportion of patients with these tumors. Accordingly, LY6K may be used in combination with other tumor markers to significantly improve the sensitivity of cancer diagnosis. LY6K may be used in the treatment of ESCC cells, as demonstrated by the fact that small interfering RNAs (siRNAs) of LY6K suppressed growth of the cancer cells. Moreover, the LY6K molecule is also a likely candidate for development of novel therapeutic approaches, such as antibody therapy.
CN103040844A Two-dimensional calcium acetate composition The invention relates to a two-dimensional calcium acetate composition, and belongs to the technical field of medicines. The composition comprises the following active ingredients in parts by weight: 100-1,500 parts of calcium acetate; 0.1-60 parts of vitamin K and 0.001-0.1 parts of vitamin D. The two-dimensional calcium acetate composition has the benefits that with the adoption of a scientific formula, calcium can be supplemented effectively; and the two-dimensional calcium acetate composition is safe and convenient to take.
US20080317737 Drug combination for the treatment of skin disorders A topical treatment for skin disorders and diseases comprising a combination of at least one antifungal agent and at least one hydroxy acid agent formulated into shampoos, creams, lotions, gels, sprays, foams, pads, films, patches, and solutions for treatment of skin disorders and diseases in both humans and animals.
US20120010170 "Methods of Reducing Nephrotoxicity in Subjects Administered Nucleoside Phosphonates" A conjugate compound comprising an acyclic nucleoside phosphonate covalently coupled to a lipid for the therapeutic and/or prophylactic treatment of viral infection in an immunodeficient subject is described, along with compositions and methods of using the same. A preferred conugate compound is CMX001, having formula (I) or a pharmaceutically acceptable salt thereof.
US20100210590 Compositions and treatments for seizure-related disorders The present invention relates to therapeutic and/or prophylactic uses of pyridazine compounds and to pharmaceutical compositions containing one or more of these compounds as an active component for treating a disorder characterized by conduction disturbances, electroconvulsions and/or seizures, in particular epilepsy, more particularly pediatric epilepsy. In an aspect of the invention, the pyridnsine compound has the Formula (Ia) or (Ib) wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the description.
EP1749007A2 Macrocyclic compounds as inhibitors of viral replication The embodiments provide macrocylic compounds, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
CN1679606A Soft capsules of azithromycin and preparation thereof A softgel of azimycin is prepared from azimycin, diluent, antioxidizing agent, solubilizer and cosolvent through dissolving gelatin in water, adding glycerine, vacuum degassing, laying aside, sequentially mixing solubilizer, diluent, azimycin and antioxidizing agent, stirring, pilling, drying and polishing.
US20100047340 Hot-melt extrusion of modified release multi-particulates The present invention includes compositions and methods of making a modified release pharmaceutical formulation and a method of preparation for the embedding of modified release multi-particulates into a polymeric or wax-like matrix. The modified release multi-particulates comprise an effective amount of a therapeutic compound having a known or desired drug-release profile. Modified release multi-particulates may include a polymeric coat or may be incorporated into particle or core material. The polymer matrix comprises a thermoplastic polymer or lipophilic carrier or a mixture thereof that softens or melts at elevated temperature and allows the distribution of the modified release multi-particulates in the polymer matrix during thermal processing. Formulation compounds and processing conditions are selected in a manner to preserve the controlled release characteristics and/or drug-protective properties of the original modified release multi-particulates.
EP1619250A1 WSX receptor and ligands The WSX receptor and antibodies which bind thereto (including agonist and neutralizing antibodies) are disclosed, including various uses therefor. Uses for WSX ligands (e.g., anti-WSX receptor agonist antibodies or OB protein) in hematopoiesis are also disclosed.
CN103435715A Preparation method and application of vanadium complexes of oligosaccharides and derivatives thereof The invention discloses a preparation method and application of vanadium complexes of oligosaccharides and derivatives thereof. The preparation method comprises the following steps: hydrolyzing polysaccharides to obtain oligosaccharides; performing complex reaction on the oligosaccharides or derivatives thereof and VO<2+> to form complexes; and removing the excessive unreacted inorganic ions to obtain the vanadium complexes of the oligosaccharides. The vanadium complexes are used for inhibiting proliferation of BEL-7402 cancer cells and inhibiting activity of the enzyme PTP1B. The invention has the following advantages: 1, the oligosaccharides and derivatives thereof can be absorbed more easily, and have better biological activity, e.g. multiple pharmacological actions such as tumor resistance, resistance to various cardiovascular diseases, virus resistance, oxidation resistance, blood sugar reduction, immunity enhancement and the like; and 2, the oligosaccharides and derivatives thereof have better reaction activity, can react with ions to form complexes more easily due to serving as ligands, and can give full play to physiological activity of the minor element vanadium and the polysaccharide derivatives, so that the actions of the both are mutually coordinated and enhanced, thus improving availability of the vanadium in living organisms.
US7015241 Appetite-stimulating agents and remedies for anorexia An appetite-stimulating agent and a therapeutic agent for anorexia, each comprising, as an active ingredient, a sulfonamide derivative or sulfonic acid ester derivative represented by the following general formula (I): wherein the ring A represents a monocyclic or bicyclic aromatic ring which may be substituted, the ring B represents a 6-membered unsaturated hydrocarbon ring or a 6-membered unsaturated heterocyclic ring containing one nitrogen atom as a heteroatom, each of which may be substituted, the ring C represents a 5-membered heterocyclic ring containing one or two nitrogen atoms, which may be substituted, W represents a single bond or —CH═CH—, X represents —N(R1)— or an oxygen atom, Y represents a carbon atom or a nitrogen atom, Z represents —N(R2)— or a nitrogen atom, and R1 and R2 may be identical or different and each represents a hydrogen atom or a lower alkyl group, or a pharmacologically acceptable salt thereof, or a hydrate thereof.
EP2586432A2 Co-crystals of Tramadol and NSAIDs like Coxibs The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
WO2007070413A1 Treatment of corneal ulcers with topical gatifloxacin Therapeutic methods for the treatment of bacterial corneal ulcers and medicaments of gatifloxacin for topical administration are disclosed herein.
US20100305163 Pharmaceutical formulations comprising nsaid and proton pump inhibitor drugs Aspects of the invention relate to pharmaceutical formulations comprising an NSAID and acid reducer drug for therapeutic purposes, and methods of preparing the same. Further aspects of the invention relate to fixed dose pharmaceutical formulations comprising naproxen, or pharmaceutically acceptable salts thereof, and esomeprazole, or pharmaceutically acceptable salts thereof.
US20050181418 Using nuclear protein (AM-1) as screening tool in diagnosing metastatic cancer Nuclear matrix proteins (NMP) which are characterized by a defined expression in tissue, particularly prostate tissue, are provided. These NMPs are useful markers in diagnosing and monitoring the stage of malignancy of a cell and treating cell proliferative disorders associated with the NMP. Also provided are substantially purified polypeptides and nucleotide sequences encoding the NMPs of the invention.
WO2006086865A3 Combi-preparation of nucleoside and non-nucleoside reverse transcriptase inhibitors for the treatment of hiv infections The present invention concerns a pharmaceutical composition comprising nevirapine, zidovudine and lamivudine in a single coated tablet. Furthermore, the invention concerns a process to prepare such a composition, the use of such a composition in the treatment of human immunodeficiency caused by HIV infection, and a method of treatment for human immunodeficienc .
CN100998593A Stable omeprazol sodium preparation for injection A high-stability freeze-dried powder injection of omeprazole sodium is proportionally prepared from omeprazole sodium, Na2EDTA and mannitol. Its preparing process is also disclosed.
US20080226598 Dendritc specific RNA viral plasmid comprising nucleotide sequences coding tumor associated for use in developing cancer vaccine; genetic vaccines Methods are provided for generating immune responses utilizing alphavirus-based vector systems.
CA2554380A1 Mecp2e1 gene The invention is a novel MECP2E1 splice variant and its corresponding polypeptide. The invention also includes methods of using these nucleic acid sequences and proteins in medical diagnosis and treatment of neuropsychiatric disorders or development disorders.
US20110301094 New tumor suppressor gene, p28ing5 This disclosure provides a novel tumor suppressor, referred to as p28ING5, nucleic acid molecules encoding this protein, and methods of making and using these molecules. Also provided are methods of ameliorating, treating, detecting, prognosing, and diagnosing diseases and conditions associated with abnormal p28ING5 expression, such as neoplasia. Kits are also provided.
CN102125521A Paclitaxel emulsion, preparation method and application thereof The invention relates to a paclitaxel emulsion, a preparation method and application thereof, belonging to the fields of pharmacology and pharmaceutics. In particular, the paclitaxel emulsion comprises paclitaxel, an oil phase and an emulsifying agent. The paclitaxel emulsion is characterized by comprising water. A paclitaxel injection provided by the invention only contains a little even no polyoxyethylene castor oil and has the advantages of safety, stability and high drug-loading rate.
WO2007047432A1 Sulfonamide derivatives as modulators of ppar Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
US7078433 FC101 and analogs as a method of treatment for cancer The present invention provides a treatment for angiogenic diseases, including solid tumors. The treatment consists of administering therapeutically active dosages of FC101, resulting in a reduction in endothelial cell proliferation and inhibition of new blood vessel formation. FC101 can also be used as a lead compound to develop other pharmacologically-active compounds, by adding or substituting different functional groups for those already present on the FC101 molecule.
EP2103305A1 Therapeutic agent for diabetic neuropathy A therapeutic agent for the treatment of diabetic neuropathy which comprises (±)-[2-[4-(3-ethoxy-2-hydroxypropoxy)phenylcarbamoyl]-ethyl]dimethylsulfonium p-toluenesulfonate of the formula (1) as an active ingredient.
US20110250282 Prolonged Release Formulations Comprising an 2-Oxo-1-Pyrrolidine Derivative The present invention relates to a pharmaceutical composition comprising Levetiracetam, Brivaracetam or Seletracetam as active ingredient, the invention relates specifically to a prolonged release formulation.
CA2434381C Naphthostyrils Disclosed are novel naphthostyrils of formula I. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such composition, and intermediates useful in the preparation of the compounds of formula I.
EP2773643A1 Pak inhibitors for the treatment of fragile x syndrome Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of Fragile X syndrome.
CN102335296A Refreshing, inflammation eliminating and pain relieving ointment The invention discloses a refreshing, inflammation eliminating and pain relieving ointment prepared from raw materials of, by weight: 3 to 20g of emu oil, 1 to 15g of a nano-grade anion solution, 1 to 18g of menthene, 0.5 to 5g of grape seed oil, 1 to 10g of vitamin B, 1 to 10g of azone, 1 to 10g of propylene glycol, 10 to 25g of dehydrated alcohol, and 30 to 50g of deionized water. The ointment provided by the invention provides functions of mind refreshing, cerebral anoxia correcting, pain relieving, inflammation eliminating, and cerebral nervous reflex activity activating. With the ointment, fatigue and sleepiness caused by long-term cerebral activities, and disasthesia caused by car-sickness or sea sickness can be relieved. Also, the ointment is convenient to use.
WO2008038692A1 Diaryl ketimine derivative A compound represented by the formula (I). (I) wherein R1a and R1b independently represent a hydrogen atom or the like; R2a and R2b independently represent a hydrogen atom or the like, or together form -CH2CH2- or the like; R3a and R3b independently represent a hydrogen atom or the like, or together form -CH2CH2- or the like; Y1 and Y2 independently represent -C(R)2- or the like; Z represents OR, NR2 or the like; R represents a hydrogen atom, a C1-6 alkyl group or the like; Ar1 represents a 6-membered aromatic hydrocyclic group or the like; Ar2 represents a 6-membered aromatic hydrocyclic group or the like; and A3 represents a 6-membered aromatic hydrocyclic group or the like. The compound is useful as a pharmaceutical agent for a central nervous system disease, a cardiovascular disease or a metabolic disease.
US7598268 Vascular endothelial growth factor; tyrosine kinase inhibitor;angiogenesis inhibitor; anticarcinogenic agents Organic compounds having the formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.
CN102145019A Medicinal composition containing truffles, vitamins and mineral substances The invention belongs to the field of medicines or health-care food, and discloses a medicinal composition containing truffles, vitamins and mineral substances. The medicinal composition comprises 0.1 to 10 weight parts of truffle mycelium powder or 0.1 to 10 weight parts of truffle extract, 0.005 to 3 weight parts of vitamins and 0.05 to 3 weight parts of mineral substances. Pharmacological experiments indicate that the medicinal composition has the excellent effect of improving immunity.
CN101129403A Medicine composite for treating dermatopathy The invention discloses a pharmaceutical composition for treating skin diseases, wherein the constituents include (by weight ratio) glycerin 80-100, camphor 9-10, salicylic acid 60-80, benzoic acid 40-60, iodine tincture 85-100 and ethanol 600-700.
WO2014127141A1 Substituted 1h-pyrazol-1,2,4-oxadiazole derivatives as sphingosine receptor modulators The present invention relates to substituted 1 H-pyrazol-1,2,4- oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-l-phosphate receptors. Claimed are compound srepresented by Formula II, its enantiomers, diastereoisomers, tautomers, or a pharmaceutically acceptable salt thereof. An example for the above Markush formula is: Example 5
US20060039959 Film-Shaped Mucoadhesive Administration Forms For Administering Cannabis Agents A film-shaped, mucoadhesive administration form having a content of at least one active agent. The active agent is a cannabis agent.
WO2006075165A1 Combination of oncolytic viruses with angiogenesis inhibitors The invention relates to a combination therapy which comprises an tumour selective toxic virus and one or more therapeutic agents that reduce tumour blood vessel formation or damage tumour vasculature, especially for use in the treatment of neoplasms including solid tumours, metastases and other vascularised lesions. The therapeutic agent or agents may have additional antitumour effects, for example, as inhibitors of tumour cell proliferation via a cell cycle specific effect or via signal transduction inhibition. Preferred therapeutic agents are angiogenesis inhibitors including mTOR inhibitors, and vascular targeting agents. Tumour selective toxic viruses for use in the combination are replication competent viruses that have bee selected or designed to replicate preferentially in tumour cells and cause tumour cell killing.
CN101953779A Medical disinfection gel The invention relates to a medical disinfection gel. The medical disinfection gel comprises the following components in percentage by mass: 1.0 to 5.0 percent of orthophenyl phenol, 55 to 65 percent of ethanol, 1.0 to 5.0 percent of thickening agent, 3.0 to 8.0 percent of humectant, 1.0 to 3.0 percent of pH regulator and the balance of deionized water. High gelling property is achieved by taking the orthophenyl phenol as a main active ingredient, taking the ethanol as a synergistic agent and adding the thickening agent, the humectant and the pH regulator. The medical disinfection gel has the advantages of reasonable formula, stable performance, convenient use, rapid cleaning, good disinfection effect, reliable effect, harmlessness to skin and no potential health risk and is particularly suitable for medical hand washing and hand wiping disinfection.
CN103463041A Application of Lycojaponicumin B in medicine for treating bladder cancer The invention discloses an application of Lycojaponicumin B in preparation of a medicine for treating bladder cancer, which belongs to the technical field of new medicine use. As shown by in vitro MTT antitumor activity evaluation, the Lycojaponicumin B disclosed by the invention also has an excellent inhibitory effect on the growth of human bladder cancer cell strain T-24. Therefore, the Lycojaponicumin B can be used for preparing a medicine for preventing bladder cancer and has a good development and application prospect. The use of the Lycojaponicumin B related to the invention in the preparation of a medicine for treating bladder cancer is disclosed for the first time, the skeleton type belongs to a brand-new skeleton type, and the inhibitory activity of the Lycojaponicumin B on bladder cancer cells is unexpectedly strong.
US20120289452 Compositions and methods for treating and preventing necrosis A method for treating and/or preventing cell necrosis and diseases associated therewith, comprising the inhibition of one or more elastase enzymes within said cells.
WO2011139791A2 Bisphosphonamidate prodrugs and uses thereof Bisphosphonamidate prodrugs of therapeutic bisphosphonate compounds and uses thereof to treat diseases are described.
US20120046518 Estrus Synchronization Preparations & Effective CIDR-Less Protocols An injectable preparation of estrogenic and progestrogenic hormonal compounds in an anhydrous excipient injected to synchronize estrus in non-menstruating placental female animals, and a five to nine day protocol to apply the unique preparation to achieve estrus synchronization.
US20120009277 Method for selection of novel anti-cancer herbs using cheminformatic tools The various embodiments herein provide a new method of selecting novel anti-cancer herbs using cheminformatics tools. The method involves collecting the herbs having synergistic activity with anti-cancer compounds and categorizing the herbs as synergistic plants (SP). The bioactive compounds are selected from the SP and categorized into synergistic compounds collection (SCC). A similarity search is performed using the selected bioactive compounds through available databases to select similar compounds that are categorized as similar synergistic compounds (SSC). A herbal source for the SSC is searched and categorized as similar herbal synergistic compounds (SHSC). The novelty of the SHSC in cancer treatment is confirmed. The novel herbs are categorized as novel candidate herbs (NCH). The synergistic activity of the resulted herbs (NCH) is confirmed by performing in vitro bioassay.
US20110086042 Centrosomal Proteins, Nucleic Acids and Method of Use Thereof The present invention provides novel isolated centrobin polynucleotides and polypeptides encoded by the centrobin polynucleotides. The invention additionally provides methods of inhibiting cell growth by contacting a cell with a centrobin inhibitor.
US20120264776 Menthol liquids composition A liquid antitussive composition comprising about 0.05 grams to about 0.2 grams of menthol per 100 ml of liquid antitussive composition, a solvent system, and a surfactant, wherein the composition has a maximum alcohol content of about 0.5 grams per 100 ml of the liquid antitussive composition, and wherein the composition is stable for about 6 months at 40° C., 75% relative humidity conditions.
CN102626408A Application of isatin thiosemicarbazone compound in inhibition of NDM-1 activity The invention provides application of isatin thiosemicarbazone compound with the following general formula (I) in preparing medicament for inhibiting activity of NDM-1. In the formula (I), R1 is selected from the group consisting of hydrogen and C5-C10 aralkyl; R2 is selected from the group consisting of hydrogen, C1-C4 alkyl and halogen; and R3 is selected from the group consisting of hydrogen and C1-C4 alkyl. The compound can significantly inhibit the activity of NDM-1.
US20080051463 Anthracene compounds and their use for treating benign and malignant tumor disorders The present invention provides novel anthracene compounds according to the formulae (I) and (II) and also selected anthracene compound compounds. The present invention furthermore provides a process for preparing such anthracene compounds. Also provided are pharmaceutical formulations comprising these anthracene compounds. The anthracene compounds provided are particularly suitable for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions which can be treated by inhibiting tubulin polymerization and/or by inhibiting microtubuli-based motor proteins, in particular various tumor disorders.
US20120195981 Micronutrient supplement with calcium, vitamin d or calcium & vitamin d combination for premenstrual syndrome, postpartum depression, depression and panic attacks A bolus dose supplement, foodstuff, beverage and beverage concentrate with calcium and vitamin D for the treatment and prevention of PMS, panic attacks, and postpartum depression. The combination of adequate calcium and vitamin D is provided as a multi-vitamin and mineral supplement. The bolus dose is comprised of 2 main ingredients calcium and vitamin D at 1000-1500 mg of elemental calcium in the form of carbonate or citrate or gluconate or citrate maleate and 400-20,000 I.U. of parent vitamin D
US7115590 Phosphoramidate, and mono-, di-, and tri-phosphate esters of (1R, cis)-4-(6-amino-9H-purin-9-yl)-2-cyclopentene-1-methanol as antiviral agents The present invention relates to phosphoramidate, and phosphate esters of (1R,cis)-4-(6-amino-9H-purin-9-yl)-2-cyclopentene-1nethanol, processes for their preparation, and their use in treating viral infections.
US20120321724 Method of Measuring and Monitoring In Vivo Nitrite Levels A method of measuring in vivo nitric oxide and nitrite levels in individuals by providing a salivary nitrite test substrate, testing salivary nitrite levels with the test substrate, measuring nitrite levels detected in the testing; and correlating the measured nitrite levels with in vivo nitric oxide bio-availability.
CA2524900C 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines The invention relates to novel 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines, process for their preparation and their use for producing medicaments for improving perception, concentration, learning and/or memory.
CN1876630A Preparation method of amorphous fluvastatin sodium The invention relates the preparing method of non-shaped fluorine-vastatin sodium. The current technology has many defects. The method comprises the following steps: preparing menthol dissolution liquid, dissolving fluorine-vastatin calcium in the liquid, distilling and getting the menthol dissolution liquid which can be recovered. The invention has the advantages of simple technology and high productivity.
EP2683709A1 Pyridinyl- and pyrazinyl -methyloxy - aryl derivatives useful as inhibitors of spleen tyrosine kinase (syk) A compound of formula (I) or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
CN101993473A Polypeptide glaucocalyxin A derivatives as well as preparation method and application thereof The invention discloses the structure and preparation method of polypeptide glaucocalyxin A derivatives as well as applications thereof in treating cancers. The general formula of the molecular structure of the polypeptide glaucocalyxin A derivatives is shown in the description, wherein R1 and R2 are -OH or a group as shown in the description, and R3 is straight-chain polypeptide substituent group. The preparation method disclosed in the invention is as follows: in the presence of tetrahydrofuran (THF) and 4-dimethylamino pyridine (DMAP), reacting extracted glaucocalyxin A with succinic acid; subsequently, in the presence of the THF and dichloroethane, reacting obtained succinic acid easter of the glaucocalyxin A with N-hydroxysuccinimide (NHS) to obtain intermediates; and finally, in the presence of the THF and phosphate buffer solution (PBS), carrying out derivatization reaction on the intermediates and the straight-chain polypeptide, thereby obtaining the polypeptide glaucocalyxin A derivatives disclosed in the invention.
EP2575807A1 Formulation based on sulpiride and a synergistic homeopathic composition for treatment of depressive syndrome The discloses involve a therapeutic formulation comprising (i) sulpiride (1); (ii) a homeopathic composition consisting of the Krebs cycle involving compounds and herbal extracts; and (iii) one or more excipients which yield in desired final dosage form: injection, tablets, capsules, oral solution, and syrup. The formulation exhibits a profound antidepressant activity due to synergistic action of homeopathic composition of Krebs cycle- involving components and herbal extracts on basic pharmacological effects of sulpiride, providing: potent antidepressant action at dosages of sulpiride up to seven times (7x) lower than is usual according to conventional clinical procedures; absence of side- effects of sulpiride due to significatly reduced dosages; as well as substantial anxiolytic and hypnotic activities.
CN101194906A Dropping pills for treating hypersensitivity disease and method for preparing the same The invention relates to a dripping pill for curing allergic rhinitis, acute and chronic urticaria, and the other allergic dermatitis. The invention overcomes the shortcomings of the prior dripping pills that pure natural degrees of findings which are used by the prior dripping pills are not high, and chemosynthesis findings which are commonly used are not in food additives catalogs of some countries, and tastes of the dripping pills are worse. The invention is a pharmaceutical preparation whose natural degree is higher, safety is stronger, and side effect is lower.
US20090156558 Phosphonate analogs of antimetabolites The invention is related to phosphorus substituted antimetabolites, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
CN103099938A Jiuhua plaster The invention provides a jiuhua plaster. The jiuhua plaster comprises 19 to 22% of talc, 3.0 to 3.3% of borax, 0.5 to 0.7% of bulbus fritillariae cirrhosae, 0.5 to 0.7% of vermilion, 4.0 to 4.4% of keel, 0.5 to 0.7% of borneol, and oil phase components serving as carriers. The jiuhua plaster is characterized by comprising edetate disodium or sodium calcium edentate, and preferably comprising edetate disodium only.
EP1690545B1 Preparation of Product R and product so obtained The present invention discloses a method of treating patients having AIDS or HIV infections by parenterally administering Product R, a peptide-nucleic acid preparation, in a combination with one or more antiviral agents useful for treating AIDS or HIV infections including HIV protease inhibitors and nucleoside analogs.
CN101843683B Inflammation-diminishing and muscle-growing oil The invention belongs to the medicine field and particularly relates to inflammation-diminishing and muscle-growing oil, which is prepared by decocting a mixed medicine by edible vegetable oil with slow fire and then filtering, wherein, the ratio of the edible vegetable oil to the mixed medicine is 3:1-5:1; the mixed medicine is prepared by mixing a heat-clearing antimicrobial drug, sanguisorba officinalis, polygonum cuspidatum, schisandra chinensis, semen strychni and borneol; and the heat-clearing antimicrobial drug is one or a mixture of coptis chinensis and radix scutellariae. The inflammation-diminishing and muscle-growing oil has simple process and low manufacture cost; treatment of diminishing inflammation, easing pain and growing muscle can be effectively carried out to a superficial wound through extracting effective ingredients of the medicine by edible oil; the oil has strong effects of antibiosis, astringency, relieving swelling and promoting wound healing, can promote thegrowth of a granulation tissue and newly born epithelium and shorten the time of wound healing, has wide indications, and can be taken as one of the standing medicine in a health-care and treating medicine box for families.
CN101565444B Circular altin type triterpene in Kleinhovia hospital as well as preparation method and application thereof The invention provides a total triterpene compound of Kleinhovia hospita, which mainly comprises five types of cycloartane triterpene compounds. The total triterpene of Kleinhovia hospita is prepared into an extract by alcohol extraction or refluxing, decompression and condensation; then the extract is arranged on macroporous resin for separation after pre-treatment; water and alcohol with concentration of 30 percent are used for eluting and removing impurities; then alcohol of 60 percent to 100 percent is used for eluting; the eluting liquid is collected and concentrated to obtain total triterpene of Kleinhovia hospita and then five types of cycloartane triterpene compounds are obtained by multi-stage chromatographic separation. The total triterpene of Kleinhovia hospita and the five types of cycloartane triterpene compounds have strong protective effects on the Hep G2 cell toxicant of a human liver cancer cell strain induced by nitrofurantion, prompts that the compounds have potential liver protection value, and can be applied for preparing drugs for protecting liver cells. The invention prepares the cycloartane triterpene compound from the Kleinhovia hospita for the first time,and provides a preparation method which is reasonably designed, as well as is simple and practical.
US20090312290 Combination of a nitrogen mustard analogue and imatinib for treatment of chronic lymphocytic leukemia The invention relates to a combination which comprises (a) a nitrogen mustard analogue selected from chlorambucil, chlornaphazine, estramustine, mechlorethamine, mechlorethamine oxide hydrochloride, novembichin, phenesterine, prednimustine, trofosfamide or uracil mustard and (b) 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of formula or a pharmaceutically acceptable salt thereof, the invention pertains to the use of said combination for the treatment chronic lymphocytic leukemia.
WO2011101866A3 Gastric retention formulation containing baclofen The present invention discloses a gastric retentive formulation (capsule or tablet) containing baclofen. Said formulation comprises an immediate and a sustained release part whereas the sustained release part is comprised in the core of the formulation and the immediate release part is present in the form of a layer which is applied on said core. The formulation is suitable for once-a-day administration.
US20100234325 4-Peroxycyclophosphamide use thereof 4-Peroxycyclophosphamide is provided along with its method of preparation. The compound is useful for treating human cancer, particularly human primary and metastatic malignant brain tumors.
CN101372499A Novel medicament having antiinflammatory activity The invention relates to an etioallocholane glucocorticoid receptor stimulant compound and a preparation method thereof. The invention also relates to medical preparation containing the compound and treating usage of the compound, in particular to the treatment on inflammatory disease, allergic disease or anaphylactic disease.
CN101278896B Chitosan nano silver gel agent and uses thereof The invention relates to a chitosan nano silver gelata used for treating an inflammation in a lower genital tract, cervicitis and cervical erosion of female and empyrosis, scalding, bedsore infection and other skin inflammations such as tinea manus and pedes, and various wound infections, etc. The medicinal raw materials of the chitosan nano silver gelata of the invention are the nano silver and chitosan polymer in respective therapy dose; the nano silver is the nano silver powder or the nano silver colloid; the chitosan polymer is the chitosan and the chitin and one or more than one derivative of the chitosan and the chitin. The product of the invention has the advantages of high efficiency and being nonpoisonous, and has an extremely strong antibacterial action and an excellent therapeutic effect; compared with other nano silver gelata, the chitosan nano silver gelata of the invention has the advantages of perfect sterilizing effect, long-lasting effect and tissue repair function.
CN1899250A Application of biological active matteri-abric ketone cellulose and its dervivative The present invention relates to the application of Alopecurone as one kind of bioactive matter and its derivative. Alopecurone is one kind of flavone compound extracted from Sophora alopecuroides or synthesized biologically. Alopecurone and its derivative have obvious function of regulating and balancing human body's endocrine and can promote the auxin secretion of anterior pituitary. Alopecurone and its derivative may be also used as multifunctional active component for cosmetics. Alopecurone and its derivative are used in treating short stature of teenagers caused by various factors, and clinical test proves their effectiveness rate up to 99.75 %.
US20060205967 Use of pamoic acid or one of its derivatives, or one of its analogues, for the preparation of a medicament for the treatment of diseases characterised by deposits of amyloid aggregates The use of pamoic acid or of one of its derivatives is described with general formula (I), in which groups R1 and R5 are as indicated in the description, or of one of their pharmaceutically acceptable salts, for the preparation of a medicament for the treatment of diseases characterized by deposits of amyloid aggregates.
US20090123535 Oral Controlled Release Formulation for Sedatives and Hypnotic Agents The present invention relates to a novel controlled release dosage form that releases therapeutic amounts of a sedative or hypnotic agent rapidly after administration and maintains therapeutic levels for about eight hours after administration.
WO2008007780A1 Pentadienamide derivative Disclosed is a pentadienamide derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof or the like. (I) wherein R1 represents a substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents a substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like; R3 represents a hydrogen atom or, together with R4 and a nitrogen atom adjacent to R3, forms a substituted or unsubstituted heterocyclic group; R4 represents a substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, or, together with R3 and a nitrogen atom adjacent to R4, forms a substituted or unsubstituted heterocyclic group; and R5, R6 and R7 independently represent a hydrogen atom or a methyl.
WO2013192097A1 Preparation, uses and solid forms of obeticholic acid The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.
US7452897 Use of substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives for the treatment of neurodegenerative diseases The invention relates to therapeutic uses of a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): Wherein R1, R2, R3, R4 and n are as defined herein. Specifically, the compounds of formula (I) are used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer's disease. The invention relates also to intermediates for the preparation of compound of formula (I).
CN102365092A Burdock fruit extract containing arctigenin at high content and process for producing same Disclosed are a burdock fruit extract containing arctigenin at a high content and a process for producing the burdock fruit extract, both of which can be used for the treatment of pancreatic cancer. Arctiin is enzymatically converted into arctigenin with ss-glucosidase, which is an enzyme occurring endogenously in a burdock fruit. The resultant product is extracted with ethanol, concentrated, and lyophilized or spray-dried. In this manner, a burdock fruit extract containing arctigenin at a high concentration can be provided.
WO2014004229A1 Phenoxyethyl piperidine compounds The present invention provides a compound of the Formula II: Formula II wherein X is: R1 is H, -CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined together form a cyclopropyl ring; or a pharmaceutically acceptable salt thereof.
WO2008001160A1 Melanin concentrating hormone antagonists The present invention relates to compounds capable of serving as moderators of human and mammalian appetite and as such provides a means for reducing body mass. The compounds of the present invention are selective against melanin concentrating hormone and do not have the pernicious side effects resulting from compounds which interact with other appetite related brain receptors.
WO2008037258A1 [2-(6-flouro-1h-indol-3-ylsulfanyl)benzyl]methyl amine for the treatment of affective disorders [2-(6-fluoro-lH-indol-3-ylsulfanyl)benzyl]methyl amine and pharmaceutically acceptable salts thereof, provided it is not the free base in a non-crystalline form are provided for the treatment of affective disorders.
US20120237616 Stabilized hypohalous acid solutions The present invention provides a stabilized hypohalous acid solution (or formulation thereof), which may be conveniently packaged for sale, or stored for later use on demand. The invention further provides methods of making the stabilized hypohalous acid solution, as well as methods of use for disinfecting mammalian tissue, including wounds and burns, disinfecting or cleansing surfaces, or treating and/or preserving food products and cut flowers, among other uses.
CA2194064C Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.
US20110213021 Compositions and methods for treating nos-associated diseases The disclosures herein provide lipoic acid salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, or injection. Such compositions may be used to treat NOS-associated diseases such as inflammatory diseases, metabolic diseases and neurodegenerative diseases.
US20080076746 Method of Treating Fish and Crustaceans With a Tellurium Based Immunomodulator A method for the direct or adjunct treatment of bacterial or fungal infections in fish and crustaceans including shell fish which is based on providing an effective amount of an organic tellurium compound in an aqueous environment to which said fish or crustaceans are exposed.
WO2013101600A1 Cinnamic acid hydroxyamides as inhibitors of histone deacetylase 8 Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activy of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
EP2401263A2 Substituted azole derivatives, pharmaceutical composition containing the derivatives, and method for treating parkinson's disease using the same Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.
US20090270503 Nutritional supplements The present disclosure relates to novel nutritional methods and compositions containing essential fatty acids which optimize embryonic, fetal and child neurological development and provides improved nutritional support for women prior to and during lactation. Further the methods and compositions improve gestational length and birth weight. The nutritional methods and compositions are also intended for use by women to optimize infant neurological development and provide improved nutritional support for women prior to, during and after lactation.
CN101125150A Application of nanometer zinc oxide in preparing medicine for treating malignant tumor The present invention relates to a usage of nano-zinc oxide in the preparation of the drugs for treating malignant tumors, which is the usage of the nano-zinc oxide in the preparation of the anti-cancer drugs or/ and the drugs for enhancing the chemotherapy sensitivity. The size of the nano-zinc oxide is less than 180 nano meters, the preferential range is 10 nano meters to 60 nano meters, and the best value is 20 nano meters. The medical hydrophilic excipients which are used conventionally are blended with the nano-zinc oxide by ultrasonic homogeneization, so as to be prepared into the capsules, tablets, powders, granules or injections and other formulations. The present invention has the effects of inhibiting proliferation and growth of the malignant tumor cells and inducing differentiation and apoptosis of the cancer cells, which can damage the protein synthesis in the tumor cells and decompose the organic matters constituting the microbes of the tumor cells by the photosensitive self-chain reaction in the tumor cells under the premise of protecting the transduction genes from being damaged by various supplements and various enzymes in the plasma or tissue cells of the body, so as to significantly improve the effect of killing microbes of the tumor cells and have great practical values in the clinical oncology.
US20120010160 Rapidly Dissolving Oral Strip of Sugar for Hypoglycemia A method of orally administering measured doses of sugar into the bloodstream for controlling glucose levels, particularly for those individuals with diabetes or those who experience difficulty maintaining healthy blood sugar levels. The method comprises providing packets of orally ingestible strips of a disintegrating matrix containing a dose of sugar to supplement food intake between meals or to rapidly increase glucose levels in an emergency situation. Hypoglycemia is a condition of low blood sugar (glucose) levels in the bloodstream, which can have varying reactions on individuals ranging from mild to severe. The disclosed matrix and method rapidly introduces sugar into the blood stream for combating a hypoglycemic reaction. The strips are easily deployable and quickly dissolve once placed on the tongue and mixed with saliva. They can be packaged in a small, easy-to-dispense, and transportable case that allows rapid use when a sugar supplement is required.
US20100226947 Articles of manufacture releasing an active ingredient The present invention relates to articles of manufacture having a formulation distributed therein, wherein the formulation comprises an active agent which manifests a desirable property when released from the articles of manufacture. The present invention also relates to methods for manufacturing these articles of manufacture, to vehicles for applying the formulation to these articles of manufacture, and to perception indicators indicating the presence and the amount of formulation comprising an active agent applied to an article of manufacture.
WO2004099213A3 Pyrrolo (1,2-b) pyridazine compounds and their use as crf-1 receptor antagonists This invention relates to substituted pyrrolo[1,2-b]pyridazine compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with CRF1, receptors, including human CRF1, receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety-related disorders such as anxiety, and mood disorders such as major depression.
WO2007073518A2 Compounds and methods for thiol-containing compound efflux and cancer treatment Methods for therapy of cystic fibrosis and other conditions such as cancer are provided. The methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e., ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments include the use of agents to modulate transport of thiol-containing compounds within the cell. Therapeutic methods involve the administration of such agents to a patient afflicted with cystic fibrosis, cancer and/or another condition responsive to stimulation of thiol-containing compound transport.
US20110280933 Epicatechin compositions and methods Provided herein are methods and compositions for treating a subject who has pulmonary damage or an injury caused by or who is at risk for an injury caused by an anti-vesicant agent. The compositions comprise cacao extracts that include a mixture of epicatechin and one or more epicatechin oligomers and a pharmaceutically acceptable carrier. Also provided are methods for fermenting cacao to enhance epicatechin and antioxidant content.
WO2013021260A3 Compounds from anisomeles heyneana The present invention describes use of compounds of formula 1 or 2 or their compositions for the treatment of leukemia and use of compound of formula 1 or its composition for treatment of infections caused due to M. tuberculosis. The invention further discloses use of compound of formula 3 for the conversion of solar energy into electric current in dye sensitized solar cells. Also, the present invention discloses a process of extraction of compounds of formula 1 or 2 or 3 from the the extract of aerial parts of Anisomeles heyneana
WO2013019058A3 Pharmaceutical composition for inhibiting cancer recurrence or metastasis The present invention relates to a pharmaceutical composition for inhibiting cancer recurrence or metastasis and a method for inhibiting cancer recurrence or metastasis using the same. The present invention identified the activity of 2-deoxy-D-glucose (2-DG, below) for the inhibition of mammosphere formation and EMT, indicating its inhibitory effect against proliferation of cancer stem cell and cancer metastasis, which has not been known hitherto. The present invention also identified that the combined use of a biguanide based antidiabetic agent or its pharmaceutically acceptable salt and 2-DG can inhibit cancer metastasis and steeply decrease cancer recurrence in comparison to the single use of said active ingredients, resulting in a superior effect in the inhibition of cancer metastasis and recurrence when the same dosage is applied. Therefore, the pharmaceutical composition of the present invention can be used to show substantially more excellent effect with less amount of each active ingredient, reducing the side effects due to the use of excess drug and due to their pharmacological action, and providing more efficacious treatment. Moreover, when it is used along with an anticancer agent to which resistance is shown, it is expected that more synergistic effect can be exhibited. Therefore, the pharmaceutical composition and method for inhibiting cancer recurrence or metastasis according to the present invention can be used very advantageously for the treatment and prevention of metastasis or recurrence of various cancer diseases.
WO2011132017A1 Pyrido[3,4-d]pyrimidinyl acetamide derivatives as trpa1 modulators Provided are pyrido[3,4-d]pyrimidinyl acetamide derivatives as Transient Receptor Potential Ankyrin (TRPA) modulators. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Transient Receptor Potential Ankyrin 1 (TRPAl). Also provided herein are processes for preparing the compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. Formula (I).
US20090227621 Naphthyridine derivatives having inhibitory activity against hiv integrase [Problems to be Solved] To provide a novel compound having antiviral activity, especially inhibitory activity against HIV integrase, a pharmaceutical composition, especially anti-HIV drug, containing the same. [Means to Solve the Problem] A compound of the formula: (wherein: R1 is optionally substituted aralkyl; R2 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for “optionally substituted” is a noncyclic group); R4 is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in “optionally substituted formylamino”, “optionally substituted carbamoyl” and “optionally substituted amino” may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.
EP0910397B1 Vascular irrigation solution and method for inhibition of pain, inflammation, spasm and restenosis A method and solution for perioperatively inhibiting a variety of pain, inflammation, spasm and restenosis processes resulting from cardiovascular or general vascular therapeutic and diagnostic procedures. The solution preferably includes multiple pain and inflammation inhibitory agents and spasm inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. Specific preferred embodiments of the solution of the present invention for use in cardiovascular and general vascular procedures also include anti-restenosis agents. The solution is introduced luminally to continuously irrigate an arterial site during an operative/interventional or diagnostic procedure for preemptive inhibition of pain and inflammation, vascular and non-vascular smooth muscle spasm, and restenosis while avoiding undesirable side effects associated with oral, intramuscular, subcutaneous or intravenous application of larger doses of the agents. One preferred solution to inhibit pain, inflammation, vasospasm and restenosis includes a serotonin2 antagonist, a cyclooxygenase inhibitor, an endothelin antagonist, an ATP-sensitive K<+> channel antagonist, a Ca<2+> channel antagonist, a nitric oxide donor, an anti-thrombin agent, a glycoprotein IIb/IIIa receptor blocker, a PKC inhibitor and a protein tyrosine kinase inhibitor.
CN102558144A Aryl urea derivatives The invention discloses aryl urea derivatives expressed by a group of general formula structures, belonging to the field of medicinal chemistry. The invention further discloses a method for preparing the aryl urea derivatives expressed by the general formula structures. The compounds disclosed by the invention have the function of a raf kinase inhibitor and can be used in the preparation of drugs for treating tumor diseases.
CN101926766A Ciclesonide foaming agent compound The invention provides a ciclesonide foaming agent compound, comprising ciclesonide taken as an active ingredient and one or more of pharmaceutically acceptable auxiliary materials and suitable for foaming agent. The content of the ciclesonide as the active ingredient is 0.05-0.2% in percentage by weight, and the volume expansion ratio of the foaming agent compound is 25-50.
US20110318431 Pharmaceutical Compositions and Methods of Treating Neurological Insults A pharmaceutical composition containing a magnesium salt and an osmotic hypertonic agent, like a mannitol, is disclosed. Also disclosed are methods of treating individuals who have suffered a neurological insult, such as traumatic brain injury.
EP2298350A2 Composition comprising an inducing agent and an anti-viral agent for the treatment of viral disorders The invention relates to novel compositions and to novel methods for the administration of compositions to a patient or to cells in vitro for the treatment of human disorders. In one embodiment, compositions contain chemical compounds that stimulate the expression of fetal hemoglobin and/or stimulate the proliferation of red blood cells, white blood cells and platelets in patients and ex vivo for reconstitution of hematopoiesis in vivo. These methods are useful to treat or prevent the symptoms associated with anemia, sickle cell disease, thalassemia and other blood disorders. In another embodiment, compositions contain an inducing agent and an anti-viral agent. The inducing agent induces the expression of a cellular or viral product, such as viral thymidine kinase, increasing the sensitivity of proliferating cells to the anti-viral agent. Typical anti-viral agents include nucleoside analogs such as ganciclovir that inhibit viral replication. Methods involve administration of therapeutically effective amounts of the inducing agent with the anti-viral agent to destroy virus-infected cells. Viral infections that can be treated include infections by herpes viruses such as Kaposi's-associated herpes virus and Epstein-Barr virus, HIV infections and HTLV infections. These compositions and methods are particularly effective against episomal and latent infections in proliferating cells. The invention also relates to novel methods for the pulsed administration of compositions to patients for the treatment and prevention of cell proliferative disorders including deficiencies such as cytopenia and malignancies such as viral-induced tumors, other forms of neoplasia and for expansion of cells for hematopoietic transplantation.
WO2004002422A3 2’-c-methyl-3’-o-l-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections The 3'-L-valine ester of β-D-2'-C-methyl-ribofuranosyl cytidine provides superior results against flaviviruses and pestiviruses, including hepatitis C virus. Based on this discovery, compounds, compositions, methods and uses are provided for the treatment of flaviviridae, including HCV, that include the administration of an effective amount of val-mCyd or its salt, ester, prodrug or derivative, optionally in a pharmaceutically acceptable carrier. In an alternative embodiment, val-mCyd is used to treat any virus that replicates through an RNA-dependent RNA polymerase.
CN1785949A Calixarene kind lean uranium discharge prometor, its preparation method and use The present invention relates to a new-type lean uranium eccritic, its preparation method and application. The invented lean uranium eccritic is a carboxylic acid functionalized calixarene derivative. It is obtained by using calixarene as mother body, making it be reacted with halogenated carboxylate under the action of alkali, then making the above-mentioned material undergo the process of hydrolysis reaction under the alkaline condition. Said invention also provides the concrete structure characteristics of said lean uranium eccritic and its application method.
WO2013074055A1 Method for restoring and rejuvenating the human body and a pharmaceutical composition for implementation thereof The invention relates to medicine, in particular to means for influencing the energetic activity of the cells in the human body, and can be used for improving health and delaying aging of the human body, for preventing age-related diseases, and for medical protection of a population exposed to the harmful effects of radiation and chemical factors of the environment; it can be used for animals for the same purpose. The novelty of the invention is that the pharmaceutical preparation is administered to a human body not more than twice a day, at any time of day, in a quantity of 5 - 10 ml of the pharmaceutical preparation, wherein the pharmaceutical preparation further comprises ingredients that function as an activator of calmodulin and an antioxidant; calcium chloride is included as the activator of calmodulin in the pharmaceutical preparation; an antioxidant from the group of SH-compounds is included as the antioxidant in the pharmaceutical preparation; dithiothreitol is included in the pharmaceutical preparation as an antioxidant from the group of SH-compounds, and the pharmaceutical composition as an aqueous solution containing oxalic acid, lithium chloride, and theophylline, additionally contains calcium chloride and dithiothreitol in the following ratio in terms of % by mass: oxalic acid: 0.25 - 4.0; lithium chloride: 0.2 - 3.1; theophylline: 0.05 - 1.1; calcium chloride: 0.2 - 3.2; dithiothreitol: 0.1 - 0.5; distilled water constitutes the remainder up to 100 % by mass.
CN101590028A Tulobuterol-containing aquogel patch and preparation method thereof The invention discloses a tulobuterol-containing aquogel patch, which comprises tulobuterol, a macromolecular framework material, a crosslinker, a crosslinking regulator, a humectant and distilled water, wherein the crosslinker is a combination of more than two organic acids; and at least one organic acid is tartaric acid and at least the other organic acid is selected from citric acid, gluconic acid, lactic acid, malic acid and malicaicd. The invention also discloses a method for preparing the tulobuterol-containing aquogel patch. The tulobuterol-containing aquogel patch and the preparation method of the invention make the cohesion of aquogel matrix so stable that the matrix avoids cloth penetration, hardening and other phenomena; the patch is proper in viscosity and insusceptible to falling off after being adhered and can be stripped without causing pains; and the method is controllable in gel time and can meet requirements for industrial large-scale production.
US20120128805 Long-lasting gustatory and/or olfactory aversion veterinary compositions for behavior modification Disclosed herein are gustatory and/or olfactory aversion compositions comprising one or more bitterants and appropriate adhesives or tackifiers, and the like, which provide a long-lasting effect. The compositions are useful for behavior modification, especially in animals, such as pets or livestock.
CN1813934A Formulation formula for treating acute-chronic purulent tympanitis The present invention relates to a medicine preparation prescription for effectively curing acute and chronic otitis medica suppurativa. Said prescription includes the following medicinal materials: 10-30 portions of calcined alum, 2-8 portions of borneol, 5-15 portions of snake slough, 5-15 portions of atractylodes root and 2-8 portions of rhubarb.
CA2389745C Method for the treatment or prevention of flaviviridae viral infection using nucleoside analogues In accordance with the present invention there is provided a method for treating or preventing a Flaviviridae viral infection in a host comprising administering a therapeutically effective amount of at least one compound of formula (I) or (II) or a pharmaceutically acceptable salt thereof, wherein Ra, R, Z and Y are defined in the application.
US7638643 Process for producing soybean saponin-containing material It is intended to easily separate saponins from isoflavones extracted from starting soybeans thereby giving highly pure saponins at a high yield on an industrial scale. Saponins can be highly efficiently separated from isoflavones by performing multistage extraction under mild conditions such that malonyl isoflavone glycoside, from among isoflavones contained in the starting soybeans, is not converted into isoflavone glycoside, acetyl isoflavone glycoside or isoflavone aglycon. Thus, highly pure saponins can be obtained at a high yield on an industrial scale.
CN103463392A Preparation method of ointment for external use The invention discloses a preparation method of ointment for external use. The preparation method comprises the following steps: taking 50 g of pepper, 60 g of leek, 30 g of aloe and 30 g of fig, cleaning and airing the components, adding 20 g of potassium permanganate, and chopping the mixture into paste for future use; and adding sodium carbonate into the obtained paste, fully stirring and uniformly mixing to obtain the ointment for external use. According to the preparation method disclosed by the invention, a variety of readily obtained materials are adopted, the effect is more significant after the materials are mixed due to the natural characteristics of the materials, a good effect can be achieved without adding any hormone substance, and the formula is mild and inirritative.
CN101698087A Quality test method of Yidan tablets The invention discloses a quality test method of Yidan tablets, comprising the steps of identifying the Yidan tablets, determining the content of chlorogenic acid and the like. Through determination by the method, honeysuckle in each tablet can not be less than 0.50mg in term of the chlorogenic acid (C16H18O9). The method of the invention features advanced technology and simple and convenient operation, and can effectively control the quality of the products.
US8067394 Synthesis and biological activities of new tricyclic-bis-enones (TBEs) This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-γ, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
WO2014023271A1 Casein kinase 1 inhibitors for the treatment of b-cell chronic lymphocytic|leukemia The invention provides new medicaments for the treatment of the B-cell chronic lymphocytic leukemia, which are inhibitors of casein kinase 1.
WO2008140081A1 Liposome and method for producing liposome It is intended to provide a liposome preparation which is a liposome, has a lipid bilayer membrane composed of an inner membrane constituted by a lipid including one or more types of functional lipids (a lipid capable of chemically interacting with another compound such as a charged lipid, a polarizable lipid, a lipid-soluble lipid or a water-soluble lipid) and an outer membrane constituted by a lipid with or without including one or more types of functional lipids, and is characterized in that at least a condition that the amount of any one type of functional lipid contained in the inner membrane is larger than in the outer membrane is satisfied. The liposome preparation is suitable as a liposome for encapsulating a contrast agent (a neutral substance having a hydroxy group), siRNA (an anionic substance) having an anticancer activity or the like. Its encapsulation ratio of drug agents, dispersion stability, control release and the like have been improved.
EP2376196A1 Animal treatment formulation and methods of use The present invention relates to a formulation for administration to the teat canal of the mammary gland of an animal, the formulation including: a physical barrier material, characterised in that the formulation includes sufficient antibiotic in relation to physical barrier material such that the formulation is configured to disintegrate over a period of time after administration to the teat canal.
US20080214654 Substituted Benzyloxy-Phenylmethylamide Derivatives The present invention relates to novel substituted benzyloxy-phenylmethylamide derivatives, processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol Receptor 1 (CMR-1) activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
WO2013191244A1 Pyridopyrimidin-4-one derivative A compound represented by formula (I) (in the formula, X represents a nitrogen atom or the formula CH; R1 represents a C1-5 alkyl (this C1-5 alkyl may be substituted by 1-3 of the same or different substituents selected from hydroxy, halogen atoms, cyano, C3-7 cycloalkyl, and C1-5 alkoxy); and R2 represents a hydrogen atom or C1-5 alkyl (at least one hydrogen atom in this C1-5 alkyl is 3H)) or a pharmaceutically acceptable salt thereof is useful as a novel [3H]-labeled ligand that binds specifically to the arginine-vasopressin V1b receptors or as a precursor for efficient [3H]-labeled ligand synthesis.
CN102526073A Application of mogrol H9 for preparing antitumor drugs The invention belongs to the technical field of chemical and pharmaceutical industry and particularly relates to the application of mogrol H9 for preparing antitumor drugs. The invention provides the application of mogrol H9 for preparing antitumor medicaments. The tumor cell can be liver cancer cell, leukaemia cell, cervical carcinoma cell, lung adenocarcinoma cell, stomach cancer cell, breast cancer cell or pancreatic cancer cell. The compound H9 is a natural product, has less toxic and adverse effects, high bioavailability and stable property, and is significant in clinical use. The small molecule compound is developed as a new antitumor drug or antitumor effective component, has an obvious antitumor effect, is green and environment-friendly, and provides a new approach to treatment and healing of tumors.
US20080233208 Administering a composition of a 3,4,5-trimethoxyl phenyl ethyl-2-methoxy-phenol; enhancing the efficacy of chemotherapeutics without adding to its toxicity This invention relates to a use of the compound of formula (I), Erianin, in preparing pharmaceutical for treating tumors
US20120328687 Formulations of selective alpha-2 agonists and methods of use thereof The invention provides compositions and methods utilizing low concentrations of selective α-2 adrenergic receptor agonists, preferably, brimonidine. The invention provides contact lens solutions and methods of using these solutions for pre-soaking contact lenses to achieve reduction of redness and/or increase in whitening of eyes. The invention also provides compositions including a selective α-2 adrenergic receptor agonist in a combination with an ocular medical device, including but not limited to a bandage lens. The invention also provides combination compositions including a selective α-2 adrenergic receptor agonist and another active agent for the treatment of an ocular condition, including but not limited to glaucoma and/or a condition associated with eye redness.
US8129362 Combination/association of adapalene and benzoyl peroxide for treating acne lesions Acne lesions, whether of inflammatory and/or non-inflammatory type, are simultaneously or sequentially treated and their number reduced, via daily topical regimen, with the combination or association of adapalene or pharmaceutically acceptable salt thereof and benzoyl peroxide (BPO).
WO2013059898A1 Pharmaceutical compositions containing sesquiterpene lactones belonging to the class of furan heliangolides for the treatment of parasitic infections and tumours One of the greatest difficulties encountered in the treatment of Chagas disease by chemotherapy is the natural resistance of T. cruzi to the pharmaceuticals available, and also the fact that parasites that are resistant to a certain compound are also resistant to other compounds. The same occurs in the treatment of cancer, where resistance to chemotherapeutic agents is daily increasing. The aim of the present invention is to provide substances having pharmacological activity and effectiveness for use as a pharmaceutical product for humans and animals, and useful for treating diseases caused by naturally resistant parasites, in particular T. cruzi and other parasites, such as those belonging to Leishmania species, and also for the treatment of cancer. The activity of furan heliangolide sesquiterpenoid compounds has been clearly verified in vivo and in vitro, in particular that of licnofolide (1), the NC-LIC presenting the best results (P < 0.005) for the treatment of infection by T. cruzi of mice infected with all the strains studied, including animals infected with the Colombian strain, which is 100% resistant to BZ, both with regard to parasitemia (CL, Y and Colombian strains) and survival of the animals (CL, Y and Colombian strains). Free lactone (free LIC9) also showed partial results for both parameters (parasitemia and survival). This confirms the previously studied activity of this lactone in vitro (Oliveira et al., Phytotherapy Research, 10(4), 292-295, 1996) and constitutes the first evidence of the potential of this substance for the treatment in vivo of parasite samples with different resistance or sensitivity profiles to drugs conventionally used for the treatment of human Chagas disease (benznidazole and nifurtimox). It was also demonstrated that the best results were observed with a formulation contained in polymeric nanocapsules obtained from PCL polymers and also from polylactic acid covalently bonded to polyethyleneglycol, the so-called stealth nanocapsules, which were described for the first time by Mosqueira et alia (Mosqueira et alia, Journal of Drug Targeting, vol. 7, no. 1, pages 65-78, 1999).
US20120309693 Methods to Accelerate Tissue and Wound Healing Rates and Reduce Swelling and Scar Formation The present disclosure serves to reduce the healing time of tissue wounds, including those formed during surgery, whether necessary or elective (including cosmetic surgery), by providing a therapeutic dose of a pancreatic enzyme inhibitor.
CA2785410A1 Tyrosine bioconjugation through aqueous ene-like reactions A new and versatile class of cyclic diazodicarboxamides that reacts efficiently and selectively with phenols and the phenolic side chain of tyrosine through an Ene-like reaction is reported. This mild aqueous tyrosine ligation reaction works over a broad pH range and expands the repertoire of aqueous chemistries available for small molecule, peptide, and protein modification. The tyrosine ligation reactions are shown to be compatible with the labeling of native enzymes and antibodies in buffered aqueous solution. This reaction provides a novel synthetic approach to bispecific antibodies. This reaction will find broad utility in peptide and protein chemistry and in the chemistry of phenol-containing compounds.
US20100074952 Tasted masked veterinary solid compositions The present invention relates to the supply and production of an animal medicine consisting of a substrate in pellet or tablet form, which is attractive to livestock and domestic animals, in which fine-grained particles of a neutral-tasting, physiologically compatible, solid carrier material are embedded, which is characterised in that said fine-grained particles of carrier material have an average diameter of 0.09 to 0.8 mm and are coated with an active substance from veterinary medicine, and said active substance layer is covered with a protective layer of a physiologically compatible polymer matrix, and to the production of this animal medicine. It also relates to the usage of said double-coated, fine-grained particles of carrier material in the production of a preparation for veterinary medicine.
WO2010125469A1 Pyrimidinedione-fused heterocyclic compounds as trpa1 modulators The present invention is related to novel pyrimidinedione-fused heterocyclic compounds as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
CN102146059A Quinazoline derivatives and preparation method and application thereof The invention discloses quinazoline derivatives serving as irreversible tyrosine kinase inhibitors, and use of the derivatives as inhibitors for human epidermal growth factor receptor (EGFR) mutant T790M and anticancer agents. The invention also relates to a preparation method for the quinazoline derivatives, and a medicinal composition containing the quinazoline derivatives.
US20100093684 Synergistic interaction of notch-1 inhibitors with glucocorticoids The present invention relates to methods and compositions for preventing and/or treating various conditions in a patient, including for example, T-cell lymphoblastic leukemia and lymphoma as well as neurodegenerative diseases, such as for example, Alzheimer's disease. In one preferred embodiment of the invention, such methods include providing a patient with an effective amount of a combination of a NOTCH-1 inhibitor and glucocorticoid. The present invention further encompasses methods for increasing the efficacy of, and mitigating resistance to, glucocorticoids in the treatment of T-cell lymphoblastic leukemia and lymphoma, which generally include providing a patient with an effective amount of one or more NOTCH-1 inhibitors.
CN101897674A L-cysteine tablet and preparation method thereof The invention relates to an L-cysteine tablet and a preparation method thereof. The tablet is prepared by rolling a pellet and comprises materials in the following percentage by weight: 30-70% of L-cysteine, 20-70% of stuffing, 1-5% of binder and 2-8% of disintegrating agent. The L-cysteine tablet prepared with the method has the characteristics of excellent stability, high bioavailability and the like. Because the L-cysteine is subjected to the oxidative degradation and is sensitive to water, in the preparation method of the L-cysteine tablet, the L-cysteine is mainly isolated from air, and water in the tablet is guaranteed within a certain range, thereby the stability of the products is guaranteed.
CA2625940A1 Use of histogranin and histogranin-like compounds as inhibitors of p2x7 receptor function and as anti-arthritic agents The invention relates to the use of Histogranin-like compounds to reduce P2X7( also designed P2Z) receptor function. The invention also provides a method for the prevention and treatment of rheumatoid arthritis and a variety of diseases/disorders including inflammatory disorders and neurodegenerative diseases.
WO2011112689A3 Salts of an indazolylpyrrolotriazine Provided herein are salts of an indazolylpyrrolotriazine, processes of preparation, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating a proliferative disease.
CN102293750B Purpose of immunological nanoparticles of brucine in preparing anti-hepatoma target drugs The invention relates to a purpose of immunological nanoparticles of brucine in preparing anti-hepatoma target drugs. The immunological nanoparticles of brucine are immunological target nanoparticles which treat brucine as an active component and a carboxylated polyethylene glycol-polylactic acid segmented copolymer as a drug coating accessory, and are formed by externally linking with anti-humanAFP monoclonal antibodies. The immunological nanoparticles of brucine provided by the invention, which have the characteristics of simple technology, high entrapment rate, stable drug release, and good balling, can be used for preparing antitumor target drugs which can be used for anti-hepatoma treatment. By intravenous injection, a nanometer carrier anti-human AFPMcAb-polyethylene glycol-polylactic acid segmented copolymer allows brucine aggregation in hepatoma cells to be increased, the drugs to be slowly and locally released, the effect time of the drugs to tumor cells to be prolonged, thelocal drug concentration to be improved, and the whole body toxicity of brucine to be reduced. So the immunological nanoparticles of brucine of the present invention have the advantages of accurate aggregation of target drugs in the cells of tumor tissues, stable drug release, good anticancer effect, safety and the like.
WO2009016350A2 Stimulating gel The invention provides a personal lubricant composition comprising a vasodilator and at least one coolant which is not menthol. Preferably, the coolant is a cyclic carboxamide such as N- ethyl-p-menthane-3 -carboxamide. In one embodiment, a second coolant is included in the composition and this is preferably (-) isopulegol.
US7384958 Quinoline inhibitors of cGMP phosphodiesterase Compounds of the formula (I) are useful as inhibitors of cGMP PDE especially Type 5.
US20090076110 An amine salt of nitric acid and aginine, beta alanine, agmatine, citrulline, creatine, glutamine, L-histidine, isoleucine, leucine,norvaline, or ornithine; vasodilation; metabolism of mucle protein;exercise An Amino Acid Compound is described. The Amino Acid Compound may comprise an Amino Acid and one of a Nitrate and a Nitrite. The Amino Acid may be one of Agmatine, Arginine, Beta Alanine, Citrulline, Creatine, Glutamine, L-Histidine, Isoleucine, Leucine, Norvaline, Ornithine, and Valine.
US20090263495 Bacteriostatic or bacteriocidal compositions and methods Particular aspects provide compositions and methods for treating or preventing bacterial infection or at least one symptom related to bacterial infection, and the like in a subject in need thereof by administering a therapeutic composition comprising at least one electrokinetically generated fluid (including gas-enriched electrokinetically generated fluids) as disclosed herein, the electrokinetically altered aqueous fluid suitable to alter cellular membrane structure or function sufficient to provide for modulation of intracellular signal transduction, wherein treating bacterial infection or at least one symptom related to bacterial infection is thereby afforded. In particular embodiments, the fluids are gas-enriched fluids or therapeutic compositions and methods, and include oxygen-enriched water optionally in combination with other therapeutic agents. Other embodiments include particular routes of administration or formulations for the gas-enriched therapeutic compositions.
WO2012127214A1 Quinolinone derivatives for use in the treatment of an autoimmune disease and/or an inflammatory disease There is provided compounds of formula I, wherein X1 to X4, R1 to R4, Y1, Y2 and L are as defined in the description, and pharmaceuticaliy-acceptable salts thereof, which may be useful in the treatment and/or prophylaxis of autoimmune diseases, inflammatory (e.g. chronic inflammatory) diseases and/or other diseases that may benefit from production of ROS (reactive oxygen species) by a NADPH oxidase complex.
WO2010084637A1 Tablet for oral administration having excellent disintegrability and dissolvability Disclosed is a tablet for oral administration, which is characterized by having a medicine layer composed of a mixture containing (A) a component selected from acetaminophen, allylisopropylacetylurea and caffeine anhydride, (B) a dried aluminum hydroxide gel and (C) a low-substituted hydroxypropylcellulose.
WO2012100342A1 Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators Disclosed herein is a compound of Formula I: wherein X, R1, R2, and R3 are as defend herein, or a pharmaceutically acceptable salt thereof to allow the drug to penetrate the cell membrane; or a prodrug, or the compound is labeled with a detectable label or an affinity tag thereof. Also disclosed is a pharmaceutical composition, a method of treating a disorder mediated by melanocortin-4 receptors, and a method of treating obesity using the compounds described.
CN101732317A Analgetic composition and application thereof The invention provides an analgetic composition and application thereof, which belong to the technical field of medicine and solve the difficult problem that the current clinical analgetic medicament has poor analgetic curative effect or large side effect. Raw materials of the analgetic composition of the invention comprise ketanserin and propranolol; and the composition can be used for preparing a medicament for treating ache. The composition of the invention has a targeted peripheral receptor and has little side effect; the components of the composition acted on different receptors can play a synergetic analgetic role; the analgetic effect is obvious; and the dosage is remarkably reduced.
WO2010122343A1 A process for the preparation of frovatriptan and frovatriptan succinate and their synthetic intermediates The present invention relates to the active pharmaceutical ingredient frovatriptan and pharmaceutically acceptable salts thereof. In particular, it relates to efficient processes for the preparation of frovatriptan and its synthetic intermediates, which are amenable to large scale commercial production and provide the required products with improved yield and purity.
EP2002838A1 Use of aryl and hetaryl amide derivatives as modulators of an EP2 receptor Use of substituted fluoro-indolyl-benzamide compounds (I) and their isomers, diastereomers, enantiomers or salts, and/or cyclodextrin clathrates, for producing a medicament to fertility control, is claimed, where (I) excludes N-[2-(7-fluoro-2,4-dimethyl-1H-indol-3-yl )-ethyl]-4-methoxy-carbonyl-benzamide. Use of substituted fluoro-indolyl-benzamide compounds of formula (I) and their isomers, diastereomers, enantiomers or salts, and/or cyclodextrin clathrates, for producing a medicament to fertility control, is claimed, where (I) excludes N-[2-(7-fluoro-2,4-dimethyl-1 H-indol-3-yl)-ethyl]-4-methoxy-carbonyl-benzamide. R 1>H or 1-6C-alkyl; R 2>H, halo or 1-6C-alkyl; R 3>SO 2NH 2, CO 2-(1-6C-alkyl), COOH, CO-NH(1-6-alkyl), CO-N(1-6C-alkyl) 2 or monocyclic 5-7C-heteroaryl, (optionally substituted with 1-6C-alkyl); R 4>H, halo, amino, OH, OCF 3, NH-(1-6C-alkyl), N-(1-6C-alkyl) 2, 1-6C-alkyl, phenyl- or naphthyl (optionally substituted with phenyl, halogen, 1-6C-alkyl, 1-6C-alkoxy, CONH 2, CO-NH(1-6C-alkyl) or CO-N(1-6C-alkyl) 2 (optionally substituted)) or monocyclic 5-7C-heteroaryl (optionally substituted with 1-6C-alkyl); and Y 1>-(CH 2) n-; and n : 1-3. [Image] - ACTIVITY : Antiinfertility; Gynecological; Analgesic; Contraceptive; Cytostatic; Osteopathic. - MECHANISM OF ACTION : Prostaglandin E2-receptor modulator. The ability of (I) to modulate prostaglandin E2-receptor was tested in immature female mice using cyclic AMP antagonist test. The result showed that N-[2-(7-fluoro-2,4-dimethyl-1H-indol-3-yl)-ethyl]-4-pyrrol-1-ylbenza mide exhibited an IC 5 0 value of 0.96 mu M.
CN102048739A Cefradine/montmorillonite composite material and preparation method thereof The invention provides a cefradine/montmorillonite composite material and a preparation method thereof. The method comprises: adding montmorillonite into deionized water, fully stirring, and dispersing under ultrasonic waves to allow water molecules to enter a montmorillonite layer fully; and adding a cefradine medicament into the solution, continuing to stir fully to allow the cefradine molecules to react with montmorillonite fully, centrifuging, collecting a precipitate, drying the precipitate, and grinding the precipitate to obtain the cefradine/montmorillonite composite material.
CN101328169B Diethylcarbamyl-substituted thiazole dihydropyrimidine The invention relates to a novel ethoxycarbonyl-substituted thiazolyldihydropyrimidine applicable to acting against hepatitis B virus (HBV) infection and a composition of the same and other antiviral agents.
WO2006097547A1 Use of 5'-methylthioadenosine (mta) in the prevention and/or treatment of autoimmune diseases and/or transplant rejection The invention relates to 5'-methylthioadenosine (MTA) and the pharmaceutically-acceptable salts and/or pro-drugs thereof, which can be used in the prevention and/or treatment of autoimmune diseases, such as multiple sclerosis (MS), and in the prevention and/or treatment of transplant rejection.
WO2008104342A1 Pharmaceutical preparation for the alleviation of endometriosis A pharmaceutical composition for the treatment of endometriosis without loss of bone density comprises a gestagenic having an antiandrogenic effect, preferably 17α-cyanomethyl-17ß-hydroxy-estra-4,9-diene-3-one (Dienogest), cyproteronacetate or chlormadinonacetate at a daily dosage which is no more than two times the dosage required to suppress ovulation, together with one or a plurality of pharmaceutically acceptable adjuvants/carriers. The pharmaceutical composition according to the invention provides both the alleviation of endometriosis and the lack of a negative affect on bone metabolism and bone density, and is simultaneously able to keep the side effects known from conventional pharmaceuticals (such as hot flashes, acne, negative affects on the lipid profile) within tolerable limits. The pharmaceutical composition is thus suitable for long-term application.
US20120219583 Nucleic acid sequences encoding expandable hiv mosaic proteins The invention is directed to a nucleic acid molecule encoding a HIV-1 polypeptide which comprises the nucleic acid sequence of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, or SEQ ID NO: 4. The invention also provides a method of inducing an immune response against HIV-1 in a mammal.
WO2006090047A1 Use of a pyrazole derivative for preparing medicines useful for preventing or treating renal diseases The invention concerns the use of a cannabinoid CB1 receptor antagonist compound, alone or combined with another active principle, derived from pyrazole, for preparing drugs useful for preventing and treating renal diseases.
WO2011072290A3 Targeted dendrimer-drug conjugates V The invention provides for dendrimer conjugates useful for liver- specific delivery of therapeutic agents. The therapeutic agent is associated to the dendrimer through a enzyme-cleavable covalent linkage.
CA2160798C Gaba-ergic modulation of eye growth A composition for the inhibition of the abnormal postnatal axial growth of the eye of a maturing animal which comprises a pharmaceutically effective amount of a gamma aminobutyric acid antagonist relatively selective for GABA B receptors in the cells of the eye, said antagonist present in a carrier or diluent suitable for ocular administration. A suitable antagonist is 2-OH saclofen.
CN101199849A Compound for medicine containing nucleoside (acid) and plant extract, preparing method and function thereof The invention relates to a medical combination containing nucleotide and plant extracts, the preparation method and purpose. The medical combination is made by combining one or more nucleotide antiviral drugs and one or more plant extracts and can be made into a compound oral preparation by mixing with pharmacy-acceptable excipient, mainly for treating virus B hepatitis. The invention takes nucleotide antiviral drugs and plant extracts as the raw material, adding certain excipient with specific type and proportion. According to the technical method introduced by the invention, a variety of oral preparations such as tablet, capsule, dispersible tablet, chawable tablet, orally disintegrating tablet, buccal tablet, dropping pill, soft capsule and so on can be prepared and developed.
WO2008001769A1 Intestinal immunity-activating substance or agent, and food, beverage and animal feed containing the same Disclosed is an intestinal immunity-activating substance or agent containing β-1,4-mannobiose.
WO2010014798A3 Pyrimidotriazinediones and pyrimidopyrimidinediones and methods of using the same The present disclosure is directed to pyrimidotriazinediones and pyrimidopyrimidinediones having a formula (I), (II), or (III), or a mixture or pharmaceutically acceptable salt or hydrate thereof, and to methods of treating cancer comprising administering the same.
CN101856498B Anti-septic shock medicine composition and application thereof The invention discloses a medicine compound which contains muscarinic receptor antagonist and cholinesterase inhibitor. The medicine compound is used for resisting infection, particularly endotoxin shock, enhances the anti-shock effect, has significant effect, has small toxic and side effect, and overcomes the side effect that the current medicine normally causes. The invention also relates to application of the medicine compound in preparing anti-infectious, in particular to anti-endotoxin shock medicine.
WO2009158446A2 Crystalline forms of ((((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonyl)(propyl)carbamoyl)oxy)methyl (4-(phosphonooxy)phenyl)acetate, method of preparation and use thereof The present invention generally relates to crystalline forms of ( ( ( (4- ( (5- (cyclopropyl carbamoyl) -2-methylphenyl)amino) -5-methylpyrrolo [2,1-f ] [1, 2,4] triazin-6-yl) carbonyl) (propyl) carbamoyl )oxy) methyl (4- (phosphonooxy) phenyl) acetate. The present invention also generally relates to a pharmaceutical composition comprising said crystalline form, as well of methods of obtaining and using the crystalline form for the treatment of inflammatory-associated diseases or disorders.
CA2841173A1 Uses of labeled hsp90 inhibitors The invention concerns various methods of using labeled HSP90 inhibitors to improve treatment of cancer patients with HSP90 inhibitors, including ex vivo and in vivo methods for determining whether a tumor will likely respond to therapy with an HSP90 inhibitor. The disclosure provides a method for determining whether a tumor will likely respond to therapy with an HSP90 inhibitor which comprises the following steps: (a) contacting the tumor or a sample containing cells from the tumor with a detectably labeled HSP90 inhibitor which binds preferentially to a tumor-specific form of HSP90; (b) measuring the amount of labeled HSP90 inhibitor bound to the tumor or the tumor cells in the sample; and (c) comparing the amount of labeled HSP90 inhibitor bound to the tumor or the tumor cells in the sample measured in step (b) to the amount of labeled-HSP90 inhibitor bound to a reference.
EP1359816B1 Combination of probiotics The invention relates to a probiotic combination comprising different combinations of lactobacilli, propionic acid bacteria and/or bifidobacteria. The probiotics are preferably combined with a suitable prebiotic to form a synbiotic. The combination of the invention can be consumed as such or combined with a suitable foodstuff or pharmaceutical product, and it is therapeutically useful for example for stimulating the immune system and for general health improvement.
CN102895621A Preparation technology and production method for integrated new formulation of turtle shell decocted pill The present invention relates to a preparation technology and a production method for an integrated new formulation of a turtle shell decocted pill, wherein the raw materials of active ingredients comprise: 12 parts by weight of turtle shell, 3 parts by weight of blackberrylily rhizome, 3 parts by weight of radix scutellariae, 6 parts by weight of radix bupleuri, 3 parts by weight of pillbug, 3 parts by weight of dry ginger, 3 parts by weight of rheum officinale, etc. The production process of the turtle shell decocted pill comprises the following steps of: supersonic air-jet crushing, alcohol-water extraction, ultrasonic crushing extraction, water decocting concentration, supersonic spray drying, nanometer grinding, high pressure homogenization, nano particle preparation and the like. According to the invention, the advantages, such as multi-synergism, multi-target, embodied by a nano-carrier coupling technique, are focused to be taken of. After the integrated new formulation of turtle shell decocted pill is subjected to scale production, the production cost can be greatly reduced, the quality of products is greatly improved and the targeting property, and the sustained and controlled release performance of the medicament are enhanced. The internal and external administration of the integrated new formulation of turtle shell decocted pill can be realized simultaneously, and the medicament can be separately taken in four time slices according to the midnight-noon ebb-flow and qi and the blood flowing rule of a human body. The integrated new formulation of turtle shell decocted pill can be further prepared into films and transdermal agents, which are respectively stuck to different parts of a human body according to the midnight-noon ebb-flow and qi and blood flowing rule of the human body, and can be directly absorbed through skin.
CN103450198A Imidazo pyrido imidazole-3-substituted benzyl acetates, and synthesis, antineoplastic activities and application thereof The invention discloses 15 kinds of imidazo pyrido imidazole-3-substituted benzyl acetates represented by the general formula I [wherein R is a side chain of L-amino acid, particularly is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2C6H5, CH(OH)CH3, CH2CO2Bzl, CH2C6H4OH-p, (CH2)3NHC(NH)NH(NO2), CH2CONH2, (CH2)2CONH2, Indole-5-yl-CH2, (CH2)2CO2Bzl or (CH2)2SCH3], discloses preparation of the imidazo pyrido imidazole-3-substituted benzyl acetates, and in-vitro and in-vivo antineoplastic activities of the imidazo pyrido imidazole-3-substituted benzyl acetates, and thus discloses clinical application prospects of the imidazo pyrido imidazole-3-substituted benzyl acetates as antineoplastic drugs.
WO2008104473A3 Pyrazolopyriidine derivatives and their use as kinase inhibitors Compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds, pharmaceutical compositions, methods of using the compounds for treatment of disease associated with p38 MAP kinase.
CN102335131A Osthole micro emulsion, osthole micro emulsion sustained-release patch and preparation method thereof The invention discloses an osthole micro emulsion which comprises isopropyl myristate, PEG-40 hydrogenated castor oil, 1-3 propylene glycol, water, osthole and borneol. The invention discloses a preparation method of an osthole micro emulsion sustained-release patch, comprising the following steps of: coating acrylate pressure sensitive adhesive on non-woven fabric, preparing a medicine reservoirlayer, preparing a dried polypropylene microporous film coated with a sustained-release solution, combining all the materials, and adding the osthole micro emulsion on the medicine reservoir layer. The invention also discloses an osthole micro emulsion sustained-release patch which is prepared by the preparation method of an osthole micro emulsion sustained-release patch. The osthole micro emulsion sustained-release patch prepared according to the invention has the advantages of strong skin penetration, faster absorption of effective components, prompt effects and lasting action time, improves the curative effect and also has the advantages of being convenient to carry, causing no pollution of clothing and the like.
US20100233257 Low dose sublingual tablets of opioid analgesics and preparation process The present invention relates to a sublingual tablet and to the method for the preparation thereof.
CN102018657A Solid dispersoid containing progestational hormone, preparation method thereof and composite comprising same The invention relates to a solid dispersoid comprising progestational hormone and at least one water-soluble carrier material, wherein the progestational hormone is dispersed into the water-soluble carrier material, and the weight ratio of the progestational hormone to the water-soluble carrier material is 1:0.3-300. The solid dispersoid has the advantages of higher dissolution rate and bioavailability, good content uniformity degree, high physical stability and high chemical stability. The invention also relates to a preparation method of the solid dispersoid and a composite comprising the solid dispersoid.
US20110229530 Pharmaceutical dosage forms for time-specific drug delivery The present invention refers to an oral dosage form intended for the time-controlled release of drugs comprising a container for one or more active ingredients optionally in admixture with pharmaceutically acceptable excipients, said container consisting of at least two parts or elements that can be joined together so as to seal the contents, at least one of said elements being composed of one or more hydrophilic polymers that undergo a decrease in the glassy-rubbery transition temperature when in contact with aqueous fluids, except for polymers with pH dependent solubility soluble only at pH values above 5, optionally in admixture with pharmaceutically acceptable excipients, the wall of the elements of the container being of such thickness as to delay the release of the contained drug with respect to the time of administration.
CN101428017A Tainuolacuo-containing medicament composition for treating peptic ulcer The invention relates to pharmaceutical composition containing tyenolrazole for treating peptic ulcer. The pharmaceutical composition is characterized in that the composition comprises the following components: at least a helicobacter pylori inhibitor and at least a gastric acid secretion inhibitor. The helicobacter pylori inhibitor is selected from penicillin, penbritin, amoxicillin, metronidazole, furazolidone, erythromycin, erythromycin and the analog thereof, gentamycin and tetracycline, and the gastric acid secretion inhibitor comprises histamine receptor antagon, H<+>/K<+>-ATP enzyme (proton pump) and/or antacid. The composition can be produced into granules, effervescent tablets, tablets, capsules, syrup, injection, suspension injection, suppositories or sustained/controlled-release preparation, oral medicines or non-oral medicines, and can achieve the purpose of preventing and treating gastric ulcer and doudenal ulcer by effectively inhibiting the growth of helicobacter pylori and gastric acid secretion.
CN101536989A Metformin hydrochloride intragastric floating sustained-release tablet and preparation method thereof The invention relates to a medicament for treating diabetes, in particular to a metformin hydrochloride intragastric floating sustained-release tablet and a preparation method thereof. By adopting a framework-type material, an aerogenic agent, a lubricant, an adhesive and other prescriptions and using a unique preparation process, the invention can overcome solve the problem that sustained-controlled-release tablets in the prior art are low in bioavailability, and provides a metformin hydrochloride intragastric floating sustained-release tablet preparation with high bioavailability.
WO2011139897A2 Reduction of alpha-tocopherol quinone α-tocopherol quinone is chemically reduced by combination with a reducing agent, such as tin (II) ion in the form of stannous chloride (SnCl2-2H20), or by chromium (III) ion, such as chromium (III) in the form of chromium chloride (CrCl3- 6H20). Purified α-tocopherol is obtained from α-tocopherol formed by reduction of an oxidized α-tocopherol, such as α-tocopherol quinone, by tin (II) ion or chromium (III) ion. Purified a-tocopherol of the invention can be administered to patients in need thereof, α-tocopherol is preserved by combination with a reducing agent.
EP2594551A1 Uses of pharmaceutical-grade ferric organic compounds The present invention discloses apharmaceutical-grade ferric organic compounds, including ferric citrate, which are soluble over a wider range of pH, and which have a large active surface area. A manufacturing and quality control process for making a pharmaceutical-grade ferric citrate that consistently complies with the established Manufacture Release Specification is also disclosed. The pharmaceutical-grade ferric organic compounds are suitable for treating disorders characterized by elevated serum phosphate levels.
CN1867325A Jelly pharmaceutical preparation containing biguanide-based medicine The invention provides a biguanide drug-containing jelly preparation of which discomfort upon administration is decreased by the control of its harshness or bitterness. In addition, the preparation has stability and excellent ability for releasing a drug in the digestive tract. The biguanide drug-containing jelly preparation of the invention is characterized by comprising a biguanide drug, an inorganic acid, and a water-soluble polymer. The jelly preparation of the invention is excellent in both stability and ability for releasing a drug, which are usually incompatible characters, particularly by the action of the inorganic acid.
CN102485215A Etodolac timed-release pellet and preparation method thereof The invention relates to the technical field of medicine and discloses an etodolac timed-release pellet and a preparation method thereof. The etodolac timed-release pellet comprises: by weight, 50 to 80% of a drug-containing pellet core, 13 to 30% of a swelling layer and 7 to 20% of a controlled-release layer. The drug-containing pellet core comprises: by weight, 40 to 80% of one or more diluents, one or more disintegrating agents and lactose, 20 to 60% of etodolac, and an appropriate amount of an alcohol aqueous solution having concentration of 80 to 100%. The swelling layer comprises 5 to 8% (w/v) of one or more super disintegrating agents, 1 to 5% (w/v) of one or more adhesives, and 100ml of an ethanol aqueous solution having concentration of 80 to 100%. The controlled-release layer comprises 3 to 6% (w/v) of a controlled-release layer material, 5 to 15% (w/w) of one or more plasticizers, and 100ml of an ethanol aqueous solution having concentration of 80 to 100%. Application time and an application dose of the etodolac timed-release pellet can be designed according to disease treatment requirements. Therefore, the etodolac timed-release pellet can be utilized for treating arthritis having time rhythm.
EP2460800A1 Substituted aminothiazole derivatives with anti-HCV activity The invention provides amino-substituted aminothiazole compounds of Formula I (Formula I) in which A is a group of the formula: and the variables R and R1 to R7 are described herein. These compounds are useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.
US7563784 substituted 1,1,4-1l6-trioxo[1,2]thiazepan-4-ylamide-derived protease inhibitors which inhibit the likes of cathepsin K; treating osteoporosis, osteo- and rheumatoid arthritis and periodontal disease; inhibiting excessive cartilage or matrix degradation The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.
US8722100 Mineral trioxide aggregate (MTA) composition and use The present application discloses a fast-setting mineral trioxide aggregate (MTA) with fluoride release for practical treatment of diseases in teeth and bone, e.g. for caries treatment and/or prevention. The cariostatic MTA contain calcia-silica-alumina cement with moderately increased tricalcium aluminate content allowing high calcium hydroxide release. The MTA composition support remineralization and biomineralization, and it is suitable for stimulation of hard tissue regeneration. MTA embodiments contain superplasticizer and nanosilicate for improved mechanical properties. The MTA compositions include optional radiocontrast and nano-enriched leachable fluorine, nitrate, strontium, and phosphate. The fast-setting MTA paste exhibits flow-to-clay-like consistency, which allows new practical applications including cavity lining, temporary restoration, bonding, and cementations in one MTA embodiment. The high calcium hydroxide and high fluoride release are suitable for caries prevention and treatment, and per se inhibition of dental symptoms.
WO2013046136A1 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formual (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
WO2010014758A1 Use of hydrogenated pyrido[4,3-b] indoles for the treatment of oxidative stress Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, and diseases of aging such as diabetes and cancer with hydrogenated pyrido[4,3-b]indoles such as dimebolin, are disclosed.
CN103599085A Aspirin enteric-coated tablet and preparation technology thereof The invention disclose an aspirin enteric-coated tablet applied in the technical field of medicine preparations and a preparation technology thereof. The enteric-coated tablet comprises a tablet core and an enteric coating layer. The tablet core comprises aspirin, a filling agent, an adhesive and a glidant. The enteric coating layer comprises an enteric material, a plasticizer, an antiadherent and water. The preparation technology includes mixing blank accessories, granulating the mixed blank accessories and drying to obtain accessory particles, mixing the aspirin and the accessory particles to obtain a totally-mixed particles; subjecting the totally-mixed particles to dry granulation to obtain intermediate particles, tabletting the intermediate particles, coating the tablet core obtained after tabletting to prepare the enteric-coated tablet, and drying the enteric-coated tablet in air. According to the tablet and the preparation technology, aqueous dispersion film is adopted for coating, thus solving latent risks of solvent residue and capability of being flammable and combustible which are produced by coating dissolution by organic solvents. The blank accessories are granulated in a wet method, thus overcoming sticky punch and tablet weight difference over-limit which are caused by tabletting in large batches and for a long time.
US20120329790 Dentinal Drug Delivery Composition The present invention is a dentinal drug delivery composition composed of cationic and/or neutral porous particles containing an effective amount of a therapeutic agent and a method for using the same to provide a dental treatment.
WO2007091719A1 Concomitant anti-gpvi antibody therapy and novel medicinal use thereof It is intended to provide: a drug for preventing or treating a disease relating to platelets or the blood coagulation system which contains, as the active ingredients, an antiplatelet agent specifically inhibiting collagen-induced platelet coagulation and/or an antithrombotic agent and aims at using these agents concomitantly, and so on; a preventive/remedy for a disease associated with vascular endothelial cell injury characterized by comprising, as the active ingredient, a substance specifically inhibiting collagen coagulation; and an inhibitor for vascular endothelial cell injury or organ injury which comprises, as the active ingredient, a substance specifically inhibiting collagen-induced platelet coagulation. Thus, it becomes possible to provide: a therapy for a disease relating to platelets or the blood coagulation system by concomitantly using an antiplatelet agent specifically inhibiting collagen-induced platelet coagulation with an antithrombotic agent; a drug, a preparation or a medicinal composition for the concomitant use; and a novel use of anti GPVI antibody as a preventive/remedy for a disease associated with vascular endothelial cell injury.
US20120039983 Amphiphilic macromolecule-lipid complexes The invention provides amphiphilic macromolecule (AM)-lipid complexes, methods of making the complexes, and methods of using the complexes.
WO2010071051A1 Melanin formation inhibitor and preparation for external application Disclosed is a melanin formation inhibitor which is safe and has a high activity. More specifically, the melanin formation inhibitor contains a compound having a germacrone-like skeleton represented by chemical formula (1) as an active ingredient. The compound can be produced by the purification from a plant such as a zedoary plant (Curcuma zedoaria Roscoe (Zingiberaceae)) or a turmeric plant (Curcuma longa [syn. C. domestica]), and has a melanin formation inhibitory activity 400 times higher than that of arbutin. The melanin formation inhibitor can be added, together with an additive such as a surfactant, a pH-adjusting agent, a water-soluble polymer, an antioxidant agent and a moisturizing agent, to a base material for a cosmetic or a pharmaceutical external preparation (wherein the base material comprises various types of oily raw materials, water, an alcohol, a polyhydric alcohol or the like) in such an amount that the content of the melanin formation inhibitor in the cosmetic or preparation becomes 0.000001 to 1.0%.
WO2013146649A1 Diquafosol-containing eye drop In a diquafosol eye drop containing a chelating agent at a concentration of 0.0001 to 1% (w/v), the production of insoluble precipitates during storage, which is usually observed in a diquafosol eye drop, and the deterioration in filtering performane during a production process (a filter sterilization process) can be prevented. In a diquafosol eye drop containing a chelating agent, the reduction in eye irritation and the improvement in preservative efficacy compared with those in a diquafosol eye drop that does not contain any chelating agent are observed. Therefore, in the present invention, stable physicochemical properties can be achieved during the course of production and distribution and during the course of storage by a patient, and the reduction in eye irritation and the improvement in preservative efficacy are observed. Particularly in a diquafosol eye drop containing a chelating agent, the deterioration in filtering performance during a production process (a filter sterilization process) is prevented. Therefore, highly efficient filter sterilization can be achieved during the course of production, which contributes to the reduction in production cost.
CN103054819A Ganciclovir for injection and preparation method thereof The invention discloses ganciclovir for injection and a preparation method thereof. The preparation is formed by regulating the pH of a solution containing ganciclovir and sodium chloride to 10.0-11.5 by adopting a pH regulator, and freezing and drying repetitively. The freeze-dried powder injection of the ganciclovir for injection has the advantages of high yield, good re-dissolubility, more stable quality and the like; change of related substances during the period of accelerated test is not obvious; and the ganciclovir for injection is safer for clinical application.
US20120108674 Injectable hydrogel for the long-term supplementation of glycerol in the skin An injectable hydrogel, includes, in weight, in a physiologically acceptable carrier fluid: 0.01 to 5% of glycerol and 0.1 to 5% of cross-linked hyaluronic acid, or one of the salts thereof; characterized in that the hyaluronic acid or one of the salts thereof is cross-linked by the formation of covalent bonds using bifunctional or polyfunctional molecules, the injectable hydrogel being sterilized in moist heat and having viscoelastic properties such that Tanδ at a frequency of 1 Hz is less than or equal to 1.10. A method for producing the hydrogel, to a kit containing the hydrogel, as well as to the use thereof in dermatology are also described.
EP2123636B1 Method for producing aminoacetylpyrrolidinecarbonitrile derivative Disclosed is a method for efficiently producing an aminoacetylpyrrolidinecarbonitrile derivative which is useful as a DPP-IV inhibitor. Specifically disclosed is a method for producing an aminoacetylpyrrolidinecarbonitrile derivative represented by the formula (2) below, which is characterized in that an aminoacetylpyrrolidinecarboxamide derivative represented by the formula (1) below is acted on by an acid, and then acted on by a dehydrating agent. (In the formula (1), A represents CH2, CHF or CF2, and R1 represents an optionally substituted secondary amino group.) (In the formula (2), A and R1 are as defined above.)
WO2010001366A1 Piperazines derivatives as proteasome modulators The instant invention relates to the use of at least one piperazine derivative of formula (I): or a pharmaceutically acceptable salt thereof, as proteasome activity modulator for the preparation of a pharmaceutical composition intended to prevent and/or treat a disease condition mediated by the proteasome activity.
US20110111046 N1-Pyrazolospiroketone Acetyl-CoA Carboxylase Inhibitors The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
CN102333757A N-acyl anthranilic acid derivative or salt thereof An N-acyl anthranilic acid derivative represented by general formula (I) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.
WO2006056783A2 Structured phospholipids for treating autoimmune and neurodegenerative diseases A method of treating a patient in need of therapy for a disease in which cyokines have become dysregulated, or are otherwise capable of modulation to provide therapeutic benefit, is provided comprising administering to that patient a therapeutically effective dose of a phospholipid comprising a phosphatidyl group esterifed with one or more fatty acyl groups, characterised in that the phospholipid has at least one fatty acyl group at the sn-1 and/or sn-2 position of the phosphatidyl group, the fatty acyl group being selected from the group consisting of Ϝ-linolenoyl, dihomo-Ϝ-linolenoyl acid and arachidonoyl.
US7504483 α-β C4BP-type recombinant heteromultimeric proteins A recombinant heteromultimeric protein including at least (a) a polypeptide fusion molecule A consisting of a C4BP α-chain C-terminal fragment and a polypeptide fragment heterologous to said α chain, and (b) a polypeptide fusion molecule B consisting of a C4BP β-chain C-terminal fragment and a polypeptide fragment heterologous to said β-chain, wherein (a) and (b) are linked in the C-terminal portion to form said multimeric protein.
CN101130544A Chemical synthesis method for epinastine The invention discloses a new chemical synthesizing method of yipisidin, which comprises the following steps: ammonifying 6-chloromethyl-11-dihyrogen-dibenz [b,e] aza to generate 6-aminomethyl-11-dihydrogen-dibenz [b,e] aza; reducing the 6-aminomethyl-11-dihydrogen-dibenz [b,e] aza into 6-aminomethyl-6,11-dihydrogen-5H-dibenz [b,e] aza; generating the product through cyanogen bromide to loop. The invention simplifies the making method with little by-product, which improves the receiving rate by 69% with high purity (HPLC. 99. 0%) for industrial manufacturing.
US20080038248 Proteins Ligands For Nkg2d And Ul16 Receptors And Uses Thereof A novel member of the RAET1/ULBP family of proteins (RAET1G) is identified and characterised and shown to bind the UL16 and NKG2D receptors with high affinity. RAET1G exhibits restricted expression in normal tissues but exhibits high levels of expression in tumours and may be differentially spliced in cancer cells to produce a soluble protein. RAET1G is also up-regulated in inflammatory diseases such as coeliac disease. RAET1G may be used as a novel marker for disease conditions including cancer conditions and inflammatory diseases.
CA2213322C Thiols to promote hematopoietic progenitor cell growth The present invention relates to methods of stimulating the growth of hematopoietic progenitor cells. In particular, it relates to the use of thiols and related compounds in stimulating the growth of hematopoietic progenitor cells in vitro and in vivo. Furthermore, the present invention relates to methods of using these compounds for the treatment of marrow failure states and immunodeficient conditions, including but not limited to myelodysplastic syndromes and acquired immunodeficiency syndrome. The figure discloses bone marrow colony formation assay.
US20100129413 Method of treating and preventing viral infections A method for treatment of a viral infection in a mammal comprising a step of administering a composition containing an amount of selenium (Se) effective to raise the serum level of the mammal to at least 15 μg/L above baseline.
CN102028674A Application of needle-leaved polyprenol in preparing medicines for preventing and treating Alzheimer disease The invention belongs to the technical field of medicines, and discloses an application of needle-leaved polyprenol in preparing medicines for preventing and treating Alzheimer disease. The needle-leaved polyprenol is obtained from needle leaves of pinaceae plants such as pinus, picea, larch, fir and cedar and the like by extraction, separation and purification. The needle-leaved polyprenol is long-chain polyterpene compound formed by 14-24 isopentene group units. Cell and animal experimental results indicates that the needle-leaved polyprenol has functions of preventing and treating the Alzheimer disease, i.e., the needle-leaved polyprenol has a protection function for damage of pheochromocytoma (PC) 12 nerve cells caused by amyloid-beta protein, and can improve the passive avoidance memory capability and space learning memory capability of demented mice. Therefore, the needle-leaved polyprenol can be used for preparing the medicines for preventing and treating the Alzheimer disease.
CN101791295B Compound monoammonium glycyrrhizinate S pharmaceutical composition and method for preparing frozen powder injection The invention belongs to the technical field of pharmaceutical preparations, in particular to a compound monoammonium glycyrrhizinate S pharmaceutical composition and a method for preparing a frozen powder injection. The composition is the monoammonium glycyrrhizinate S frozen powder injection and comprises the following components: monoammonium glycyrrhizinate S, cysteine hydrochloride, glycine,anhydrous sodium sulphite, sodium citrate, sodium chloride, sodium hydroxide and water for injection. The frozen powder injection is more stable and safer.
CN102452998A N-formyl hydroxylamine compound and its preparation method and use The invention relates to an N-formyl hydroxylamine compound and its preparation method and use. The invention provides the N-formyl hydroxylamine compound shown in the formula I or an enantiomer of the N-formyl hydroxylamine compound or a racemic mixture of the N-formyl hydroxylamine compound, wherein X represents O or S; R1 represents H, a C1-C5 linear chain or a branched chain alkyl group; R2 and R3 independently represent H, a C1-C5 linear chain alkyl group, -OR', -SR', -halogen, -CN, -CONR', -COOR' or -COR'; and R' represent H, a C1-C5 linear chain or a branched chain alkyl group.
WO2011156780A3 8-(sulfonylbenzyl)pyrido[2,3-d]pyrimidin-7(8h)-ones for the treatment of cns disorders Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.
WO2008068174A1 4,5,6,7-tetrahydro-thieno [2,3-c] pyridines as h3 modulators The present invention relates to compounds of formula (I), wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
CN102579454A Drug composition for curing tumour diseases The invention discloses a drug composition for curing tumour diseases, which comprises fixed dose of N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide or pharmaceutically acceptable salt of the N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide and erlotinib or pharmaceutically acceptable salt of the erlotinib or comprises fixed dose of N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide or pharmaceutically acceptable salt of the N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide and gefitinib or pharmaceutically acceptable salt of the gefitinib. A method for preparing the drug composition and an application of the drug composition in preparing drugs for curing tumour diseases are further provided.
CN201676085U Self-heating indomethacin patch The utility model discloses a self-heating indomethacin patch which comprises a fixed layer. A heating layer is arranged on the fixed layer; a TDP coating layer is arranged on the heating layer; and an anti-bacteria layer is arranged on the TDP coating layer. The self-heating indomethacin patch skillfully applies heating agents to the structure of a treatment patch, fully plays the thermal application physical therapy effect of the heating agents to a human body and is also easier to popularize and apply due to the existence of an adhesive tape or a magic tape and other portable fixed structures. Because anti-bacteria cloth has the effects of anti-bacteria and disinfection, the self-heating indomethacin patch has more functions, greatly improves the use value of a single product, saves limited resources for the society and has great social benefit and economic benefit.
CN1965852A Aloeresin D and effective component, preparation process, pharmaceutical composition and use thereof The invention relates to a method for preparing the effective component aloe glycosides D of aloe, and relative derivant, wherein said aloe glycosides D and derivant have better beta-secretory enzyme restrain activity and nerve cell protect activity, which can be used in the drug that treats senile dementia. The effective component AC (the aloe glycosides D content is 30-50%) of aloe can be extracted via 95% alcohol, the extractive can be washed by porous adsorption resin and different alcohol solution, to recycle the solvent.
US20060252784 Imidazo-substituted 1,8-naphthyridinylamines; treating arthritis, Crohn's disease, Alzheimer's disease, irritable bowel syndrome, adult respiratory distress syndrome, and chronic obstructive pulmonary disease. The present invention discloses compounds corresponding to formula I: wherein A, Z, Z1, Y, R1 and R2 are as defined in the specification, as well as pharmaceutical formulations, methods of making and uses thereof.
CN101485645B Elemene transdermal agent and preparation method thereof The invention belongs to the field of pharmaceutical, and relates to an elemene transdermal agent, which consists of three parts of a backing layer, a medicine containing ointment and a covering layer, wherein the medicine containing ointment is prepared from auxiliary materials such as elemene, a binder, a bulking agent, a transdermal promoter, a humectant and the like according to a certain blending ratio. The transdermal agent can continuously and stably release the medicines within the scheduled time, and the blood concentration is stable, thereby fundamentally eliminating the problems ofshort effective time, frequent administration and more untoward reactions existing in the prior formulations of the elemene medicines in aspect of treating cancers. The medicine containing ointment of the transdermal agent has good compatibility and adhesive capacity with skin, and the transdermal agent is good in stability. The method for preparing the transdermal agent is simple and convenient to operate.
CN101797226A High oxidation resistance medium/long chain fat emulsion injection and preparation method thereof The invention provides high oxidation resistance medium/long chain fat emulsion injection (C8-C24) and a preparation method thereof. The fat injection consists of soybean oil for active component injection, median chain triglyceride oil, emulsifier, isoosmotic adjusting agent, metal ion chelation agent and water for injection. The method comprises the following steps: under inert gas environment, adding the emulsifier and the coemulsifier into the heated soybean oil for injection and the median chain triglyceride oil, and uniformly stirring the mixture at high speed serving as oil phase; uniformly mixing the isoosmotic adjusting agent and the metal ion chelation agent with proper water for injection, and filtering the solution serving as water phase; in high speed stirring, combining the oil phase and the water phase, continuously stirring the mixture to foremilk at high speed, adjusting the pH of the foremilk to be between 9.0 and 10.0, adding the water for injection to the volume of 1,000ml; homogenizing the foremilk after the foremilk is uniformly mixed by a high pressure homogenizer until the milk particles are qualified; and preparing the medium/long chain fat emulsion injection through filling, nitrogen introducing, plugging, capping, sterilizing and cooling after filtration.
CN102631364A Application of lincomycin in medicine for treating meniscus injury The invention relates to medicine for treating meniscus injury, and also relates to sodium hyaluronate and lincomycin as well as the application of the lincomycin in the medicine for treating meniscus injury. The medicine for treating meniscus injury is characterized by comprising the lincomycin, wherein the lincomycin is a common fungistat in the prior art and can perform the action on fighting bacterium and diminishing inflammation. The medicine for treating meniscus injury finds that the lincomycin has the action on repairing a meniscus cell, and therefore the medicine for treating meniscus injury can serve as the medicine for repairing the meniscus injury and has a good curative effct. The medicine for treating meniscus injury is combined with the sodium hyaluronate and hexadecadrol, and has a better curative effect. The sodium hyaluronate serves as a nutrient substance to simultaneously perform the action on providing articular cavity pressure, supporting joint movement and lubricating joints, and is also convenient for dispersing other medicines, such as lincomycin. The hexadecadrol has the action on enhancing the medicine effect of the lincomycin. Several medicines are cooperated to perform a better treating effect.
WO2012143860A1 Ameliorating cognitive decline A method of ameliorating cognitive decline or a related condition, comprising oral administration of an effective amount of one or more compositions of mixed phospholipids and use of a mixed phospholipid composition in the manufacture of an oral formulation for ameliorating cognitive decline or a related condition.
US20080193385 Compositions and methods for treating neuropathy The present invention relates to compositions and methods for alleviating the painful symptoms due to neuropathy. Specifically, the method involves administering to a patient a composition comprising a nitric oxide donor that may be applied topically on the legs or arms to alleviate the negative effects due to neuropathy.
WO2011121629A1 Indolic derivatives and use thereof in medical field The present invention concerns indolic derivatives and use thereof in medical field. Particularly, the invention concerns 3-[(3',4',5'- trimethoxyphenyl)thio]-1 H-indole derivatives and bioisosteric derivatives thereof and their use for the treatment of tumours.
EP1757590A1 Piperazinylalkylpyrazole derivatives useful as selective T-type calcium channel blockers and preparation method thereof The present invention provides for novel piperazinylalkylpyrazole derivatives, the preparation method thereof and the selective T-type calcium channel blocking activity thereof. Particularly, it provides a piperazinylalkylpyrazole derivative as represented by the formula set forth below or its pharmaceutically acceptable salts, and its preparation method thereof. The compound of Formula 1 is a novel piperazinylalkylpyrazole derivative, which particulary has T-type Ca2+ channel blocking effect and thus can be useful as a therapeutic agent for nerve and muscle pain.
EP2146989B1 Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH2, CH2-CH2, CH2-NH, or NH; R1 is halogen, or R1 is alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkyl, alkoxycarbonyl, aryl, all of which are optionally substituted; R2 is hydrogen, or R2 is alkyl, cycloalkyl, alkoxy, heterocycloalkyl, aryl, heteroaryl, alkoxycarbonyl, aminocarbonyl, amino, all of which are optionally substituted; A is aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocycloalkyl or heterocycloalkenyl, all of which are optionally substituted; and pharmaceutically acceptable salts, hydrates, or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments, in particular for the treatment of dermal diseases.
US20090143360 Oxcarbazepine Formulation The present invention relates to novel uncoated, color-stable tablet formulations comprising oxcarbazepine, a disintegrant and iron oxide pigments. The oxcarbazepine of the present invention has a particle size of about 14 to about 30 microns with a maximum residue on a 40 micron sieve from about 10% to about 35%. The present invention further provides for a process of preparing the tablet formulations, and a method of treating mammals in need of oxcarbazepine with the novel formulation.
CN101775007A Tricyclene compounds with HIV antagonistic activity and preparation method and application thereof The invention discloses tricyclene compounds with HIV antagonistic activity and a preparation method and application thereof. A structural formula of the tricyclene compounds is shown as a formula I, wherein R is alkyl, a naphthenic group, heteroaryl, substituted alkyl, substituted phenyl or substituted heteroaryl; and a substituting group of the substituted alkyl is any one of an alkoxyl group, a substituted or unsubstituted phenoxy group, a naphthenic group, heteroaryl, a substituted naphthenic group, substituted heteroaryl and substituted amido. An in-vitro HIV-1 infected cell model tests the activity and shows that the compounds are superactive HIV antagonists, can be used as inhibitors for inhibiting replication of HIV virus, and can be developed into anti-AIDS medicaments.
CN103655582A Epoxide sterol composition, and preparation and application thereof The invention provides an epoxide sterol composition comprising epoxide sterol A and epoxide sterol B, of which the total content is greater than 95%. The epoxide sterol composition is prepared by percolation extraction, concentration and column chromatography isolation purification of a marine animal, namely green sea anemone. Experimental results show that the epoxide sterol composition (ESC) remarkably refrains the growth of rat glioma cells C6 and human glioma cells U251, induces tumor cell apoptosis or necrosis, and can be used for preparing medicines for curing brain gliomas.
CN102824352A Application of disaccharide compound in preparing anti-tumor medicine The invention provides application of a disaccharide compound shown by the formula 1 in preparing an anti-tumor medicine. In the invention, the structure of the compound of the formula 1 is similar to that of sucrose, and the compound is a simple disaccharide compound; after entering the body, the compound shows relatively strong biological activity, can effectively suppress the tumor growth, andrealizes an obvious anti-tumor effect; the compound can enhance the immunity of normal organisms as well as organisms suffering cancers; and when in chemical therapy, the compound can improve the immunologic function of patients in chemical therapy so as to improve the quality of life of the patients suffering cancers.
CN103254127A Glycine-reuptake inhibitor and application thereof The invention relates to a glycine-reuptake inhibitor and an application thereof. The glycine-reuptake inhibitor is a compound as shown in a formula I, or an isomer, a pharmaceutically acceptable salt or solvate of the compound as shown in the formula I, wherein R1 is one or more of the following groups: hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitryl, cyanogroup, amino, hydroxyl, halogenated C1-C6 alkyl and halogenated C1-C6 alkoxy; R2 is selected from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, halogenated C1-C6 alkyl and halogenated C1-C6 alkoxy; each of R3 and R4 is independently selected from hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitryl, cyanogroup, amino, hydroxyl, halogenated C1-C6 alkyl and halogenated C1-C6 alkoxy. The compound disclosed by the invention is an efficient glycine-reuptake inhibitor.
CN102552996A Personal lubricant The invention provides a personal lubricant which is characterized in that the personal lubricant comprises a plant extract with a testosterone-like effect or a plant extract with a testosterone-like effect and a plant extract with a estrogen-like effect. Compared with the existing common products, the personal lubricant has the advantages that functions of the personal lubricant are further enriched, sex hormone can be more thoroughly supplied to women, the personal lubricant has a balancing action on the hormone of women, sexual life quality of women can be further improved, and the personal lubricant does not have toxic or side effects and dependence.
US20100222416 Diagnostic Marker and Therapeutic Target for Cancer The present invention, in general, relates to use of nm23H1-B gene for diagnosing cancer susceptibility and metastatic progression in colon/colorectal cancer. In particular, the present invention relates to identifying the alteration in the expression of nm23H1-B gene on treatment with chemotherapeutic agents for diagnosing cancer susceptibility and metastatic progression in colon/colorectal cancer.
US20080153814 8-Chloro-2,3-Benzodiazepine Derivatives The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I), wherein R stands for a lower alkyl group or a group of the general formula —NH—R′, wherein R′ stands for a lower alkyl or a lower cycloalkyl group), and pharmaceutically acceptable acid addition salts thereof. The invention also encompasses a process for the preparation of said compounds, pharmaceutical compositions containing them and new intermediates useful for the preparation of the new 8-chloro-2,3-benzodiazepine derivatives. The compounds according to the invention possess AMPA/kainate receptor inhibiting activity.
EP2400952A2 Composition of a liposomal gel containing hydrocortisone, its metabolites, precursors or mixtures thereof and the use thereof Liposomal gel which, apart from liposomes and a continuous phase, comprises at least one thickening agent, at least one biologically active material and, optionally, at least one additive, whereby the biologically active material is encapsulated in the liposomes, and whereby this material consists of hydrocortisone, its metabolites or precursors, or a mixture thereof, and is applied on the skin for therapeutic purposes, characterised in that the weight ratio phosphatidylcholine/hydrocortisone amounts to at least 2/1 and/or in that the weight ratio phosphatidylcholine/carbomer hydrogel amounts to at least 20/1.
US20100092550 Alka-eeze A composition for providing relief from acidity. The composition comprises sodium bicarbonate for use in neutralizing acids. There is one of a capsule and a tablet for enclosing the sodium bicarbonate therein, such one of such capsule and such tablet being a delayed release and a timed release system so as to delay the dissolution of the sodium bicarbonate until the sodium bicarbonate is in one of a small intestine and a large intestine.
WO2011003194A1 Oncolytic viruses and methods for treating neoplastic disorders The disclosure provides mutant ribonucleotide reductase strains of poxviruses including for example vaccinia viruses. The disclosure also provides methods and for the use of these mutant ribonucleotide reductase strains of vaccinia viruses in oncolytic virotherapy.
CN102935077A Bionic lovastatin nano-structured lipid carrier and preparation method thereof The invention relates to the field of pharmaceutical preparation, and in particular relates to a bionic lovastatin nano-structured lipid carrier and a preparation method thereof. The method is characterized in that endogenic lipid material is adopted so as to encapsulate medicines in the carrier, so that injection for intravenous injection can be produced. The prepared nano-structured lipid carrier has good biocompatibility and is biodegradable, and toxic and side effects are reduced; the bionic lovastatin nano-structured lipid carrier has small grain size, high dispersity, good stability and can long-lastingly and slowly release medicines; and lovastatin medicines and the bioactive lipid carrier can be combined together so as to achieve a collaborative treatment function, and the curative effect of the medicine in treating cardiovascular disease is increased.
US20130023568 Benzimidazole Derivatives And Their Pharmaceutical Compositions And Uses The present invention relates to benzimidazole derivatives and their pharmaceutical compositions and uses, specifically to benzimidazole derivatives of Formula (I), or their stereoisomer, pharmaceutically acceptable salt or solvates thereof, in which R1, R2, R3, R4, R5 and n have the definitions in the description; the present invention further relates to a pharmaceutical composition containing the compounds, methods for preparing the compounds, and use of the compounds for manufacturing of a medicament for prophylaxis and/or treatment of peptic ulcer, ulcer hemorrhage and diseases associated with gastric acid.
US7534800 pyrrolo[2,3-b]pyridine derivatives; treatment of neurodegenerative disorders related to apoptosis and/or inflammation; compound prepared by condensation, halogenation, hydrogenation, using silan protected drivatives The present invention relates to novel 3,5-substituted 7-azaindole compounds of formula (I), their use in the inhibition of c-Jun N-terminal kinases, their use in medecine and particularly in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation. The invention also provides processes for manufacture of said compounds, compositions containing them and processes for manufacturing such compositions.
CA2828255A1 Protein nanocarriers for topical delivery The invention encompasses nanoparticle assemblies and methods for preparing nanoparticle assemblies and compositions comprising such assemblies. The invention further encompasses methods of complexing various molecular and cellular entities to the nanoparticles using the resulting nanoparticles of the invention as delivery devices. The nanoparticle assemblies can be used for a variety of applications, such as treating cancer, targeting tumors, reducing the toxicity of a drug in vivo, increasing the efficacy of an complexed agent in vivo, protecting an complexed agent against degradation, and enhancing the water solubility of a drug or other agent.
CN101889679A Composition with disintoxicating and liver-protecting effects and application thereof in food and health-care food The invention relates to a composition with disintoxicating and liver-protecting effects, which comprises the following raw materials in percentage by mass: 0.15 to 5 percent of crucumin, 0.04 to 1.0 percent of zinc lactate, 10 to 50 percent of glutamine, 10 to 50 percent of alanine and 10 to 50 percent of xylooligosaccharide. It is proved that, by an animal experiment and a human tasting experiment, the composition increases the alcohol dehydrogenase and acetaldehyde dehydrogenase content of a body and rapidly decomposes alcohol, so that the composition has the effects of promoting alcohol metabolism in a liver and reducing the alcohol concentration and active oxygen concentration in a blood; and the composition increases an endurance capacity of a human body to the alcohol, reduces the discomforts such as headache, nausea, vomiting and the like due to the alcohol, and reduces the damages of the alcohol to the liver. The composition can be prepared into food and health-care food with the disintoxicating and liver-protecting effects, can be used as a disintoxicating product for preventing and improving excessive drinking, and can be used as an adjuvant therapy product for an alcoholic liver, a fatty liver due to the alcohol or non-alcohol and protecting the liver; and the composition has the advantages of safety, non-toxicity and a reliable curative effect.
CN102579481A Medicinal composition for treating catarrh symptom The invention provides a medicinal composition for treating a catarrh symptom. Every 100ml or 100g of the composition comprises 3-20g of montmorillonite, 0.05-0.5g of sodium hyaluronate and the balance of medicinal auxiliary materials and water. The nasal cavity of a nasal cavity administration patient is not dry, no blocky objects are formed in nostrils, and the compliance of the patient is high; the montmorillonite is not dry, the effective time is long, and the administration times are reduced; and the medicinal composition has the advantages of quick response, capability of shortening the curative course and no toxic or side effect.
US20120003307 Levetiracetam controlled release composition The present invention is concerned with controlled release compositions for oral administration comprising levetiracetam; and with processes of preparing such controlled release compositions.
CN103396435A Dibutyl tin aromatic aldehyde condensed arylamine Schiff base complex as well as preparation method and application thereof The invention discloses a dibutyl tin aromatic aldehyde condensed arylamine Schiff base complex which has a structural formula (I) as shown in the specification, wherein Bu represents normal butyl, R1 is -OCH3, -Cl or -H, R2 is -H, -Cl or -Br, and R3 is -H or -NO2. The invention further discloses a preparation method of the dibutyl tin aromatic aldehyde condensed arylamine Schiff base complex and an application of the dibutyl tin aromatic aldehyde condensed arylamine Schiff base complex for preparing medicines for treating cervical cancer, breast cancer, liver cancer, colon cancer or lung cancer.
US7479486 Sulphur analogues of 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) for treating excess of glucocorticoids The present invention is related to novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues, their use as antiglucocorticoids for the treatment and/or prophylaxis of disease associated to an excess of glucocorticoids. In particular, the invention relates to the use of novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues for treating Cushing's syndrome, iatrogenic hypercortisolism or depression. Also the present invention is related to methods of preparing the novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues.
US20120107252 Method for forming cyclodextrin polymer and lipophilic compound emulsions, resulting emulsions, and compositions including said emulsions The present invention relates to a method for preparing a cyclodextrin polymer and/or a hydrophilic polymer emulsion having cyclodextrins as well as lipophilic compounds, the emulsions having a remarkable stability. In particular, the method includes: (i) adding a lipophilic compound into an aqueous solution of a cyclodextrin unit polymer or hydrophilic polymer having cyclodextrins; (ii) forming an emulsion from the mixture resulting from step (i). The invention also relates to the resulting emulsions, i.e. stabilized emulsions by a non-covalent and non-crystalline inclusion complex consisting of (i) a cyclodextrin unit polymer or a hydrophilic polymer having cyclodextrins and (ii) a lipophilic compound. The invention also relates to the use of said emulsions in the cosmetic, pharmaceutical and/or agri-food fields.
US20050148661 calcium is in gluconate, chloride, bromogalactogluconate, gluconolactate or carbonate form, and the magnesium is in sulfate or pidolate form The invention relates to products comprising calcium, injectable magnesium and an injectable product which releases oxalate during the metabolism thereof as a combination that can be used for simultaneous, sequential or separate administration in anticancer and antiviral therapies.
EP2459554A2 Substituted benzamide derivatives as glucokinase (gk) activators The present invention relates to substituted benzamide derivatives of the general Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.
CN102532137A 8-pyrazole substituted xanthine A2B adenosine receptor antagonist and synthesis method and application thereof The invention relates to a 8-pyrazole substituted xanthine A2B adenosine receptor antagonist and a synthesis method and an application thereof. The structural formula of the A2B adenosine receptor antagonist is shown in the specifications, and the antagonist is synthesized by taking 1,3-dialkyl-5,6-diaminouracil and nitrobenzyl pyrazole-4-formic acid as raw materials and improving a Traube reaction. The synthesis method disclosed by the invention has mild conditions, low cost and high yield, is easy to operate, and is suitable for industrial production. As proved by a pharmacological experiment, the affinity and selectivity of an A2B receptor are enhanced due to substitution of the 8-position of xanthine in 8-pyrazole substituted xanthine with nitrobenzyl pyrazole, the secretion of IL-8 can be suppressed, and the release of inflammatory factors is reduced. The receptor antagonist is suitable for treating bronchial asthma.
CN102079724A Ethylene sulfonyl chloride azole compounds with anti-microbial activity as well as preparation method and medical use thereof The invention relates to ethylene sulfonyl chloride azole compounds with anti-microbial activity, and preparation of pharmaceutically acceptable salts thereof; and the invention further relates to an application of novel ethylene sulfonyl chloride azole compounds and salts thereof in the aspect of anti-infection medicaments. The ethylene sulfonyl chloride azole compounds show very valuable pharmacological activity in antibacterial and antifungal activity aspects. The general molecular formulas of the novel ethylene sulfonyl chloride azole compounds are as shown in I-X disclosed in the specification, wherein Ar, R, X, M, Im1 and Im2 are defined in the claims.
CN102247549A Prescription for treatment of epistaxis The invention aims to provide a prescription for treating epistaxis. The prescription mainly comprises: 20g of scutellaria, 10g of gardenia, 20g of lotus leaf, 10g of schizonepeta, 20g of hairyvein agrimony, 30g of rhizoma imperatae, and 20g of gypsum. A dose of the prescription can be decocted with water and taken twice every day.
WO2006006722A1 Method of controlling cell functions It is intended to provide methods of screening a gene participating in cell regeneration, proliferation and differentiation and a cell regeneration-, proliferation- and differentiation-controlling agent; a cell regeneration-, proliferation- and differentiation-controlling agent; and so on. More specifically speaking, it is intended to provide a method of screening a gene participating in cell regeneration, proliferation and differentiation which involves the step of quantitatively analyzing in a mass the expression amounts of multiple genes in cells capable of regenerating, differentiating and proliferating to thereby specify a gene participating in cell regeneration, proliferation or differentiation of the cells; a method of screening a cell regeneration-, proliferation- and differentiation-controlling agent which involves the step of quantitatively analyzing in a mass the expression amounts of multiple genes in cells capable of regenerating, differentiating and proliferating to thereby specify one or more genes showing larger expression amounts in the cells or showing specific expression compared with other cells, and the step of contacting at least one candidate substance capable of controlling the functions of the specified gene(s) or gene product(s) thereof with the cells and comparing the change before and after the contact; and so on.
US7582635 Benzoazolylpiperazine compounds inhibition of gluatmate receptors; for treatment of urinary incontinence, ulcers, irritable-bowel syndrome, inflammatory-bowel disease, addictive disorders, Parkinson's disease, parkinsonism, anxiety, epilepsy; kits A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.
US20100216842 Narcotic Emulsion Formulations for Treatment of Cancer Pain Methods and compositions of treating a subject for cancer pain are provided. In the subject methods, a subject is treated for cancer pain by administering to the subject an effective amount of a narcotic emulsion, e.g., fentanyl elmulsion, formulation. In certain embodiments, the emulsion formulations include a narcotic active agent, oil, water and a surfactant. Also provided are methods of making the subject emulsion formulations as well as kits that include the emulsion formulations.
CA2225628C Oral pharmaceutical compositions with delayed release of reversible proton pump inhibitors An oral pharmaceutical composition of a reversible proton pump inhibitor in pellet or tablet form, wherein the reversible proton pump inhibitor is at least partly in slow-release form, is distinguished, on combined administration with an antimicrobially-active ingredient, by an enhanced action of rapid onset against disorders caused by Helicobacter.
WO2014135460A1 Use of (rs)-s-cyclopropyl-s-(4-{[4-{[(1r,2r)-2-hydroxy-1-methylpropyl]- oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide for treatment of specific tumours The invention relates to the use of (R)-S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2- hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}- phenyl)sulfoximide and/or (S)-S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2- hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}- phenyl)sulfoximide for treatment of specific tumors.
CN102838545A Crystalline form IV of celecoxib, preparation method and purpose thereof The invention relates to a crystalline form IV of celecoxib and a preparation method thereof, and further relates to a pharmaceutical composition prepared by using the crystalline form IV of celecoxib obtained by the invention, and an application of the pharmaceutical composition. The crystalline form IV of celecoxib is characterized by an x-ray powder diffraction pattern spectrum, a differential thermal analysis spectrum and an infra-red spectrogram thereof.
US20060189689 Arginine mimetics as factor Xa inhibitors The invention relates generally to a novel type of arginine mimetics which are inhibitors of factor Xa; to pharmaceutical compositions which comprise these mimetics; and to the use of these arginine mimetics for producing compositions for antithrombotic therapy.
EP1762235A1 Orally adminstered composition for preventing neonatal hemorrhages, in a tardy form, caused by a K-vitamin deficiency The present invention relates to an orally administered compound, for preventing neonatal hemorrhages, in a tardy form, caused by a K-vitamin deficiency, comprising K1 vitamin, in an oil solution, to be administered in daily microdoses.
EP2161266A1 Benzofuran derivatives as orexin receptor antagonists The invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meaning as cited in the description and the claims. Said compounds are useful as Orexin Receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
CN102036714A Anhydrous and hydrate forms of crystalline 2- ( (2s, 3r, 4e, 6e, 1oe, 12s) -13- (4-fluorophenoxy) -2,3, 12- (trihydroxytrideca-4, 6, 10-trien-8-ynyl) oxy) acetic acid This invention is directed to a crystalline acid of a lipoxin A4 analog in an anhydrous form which exhibits characteristic peaks at d = 20.48 A and at d = 4.34 A and in a hydrate form which exhibits characteristic peaks at d = 9.8 A and at d = 4.6 A.
US7384983 R-(-)-N-methyl 3-((2-methyl-4-hydroxyphenyl)oxy)-3-phenyl-1-aminopropane or its hydrochloride salt; inhibiting the uptake of norepinephrine and serotonin; antidepressants, analgesics; treating sleep disorders, autism, psychological disorders, eating disorders The present invention provides compounds and methods for the inhibition of monoamine uptake in mammals.
CN101947203A Valnemulin hydrochloride emulsion for animals and preparation method thereof The invention discloses valnemulin hydrochloride emulsion for animals. Each 100ml of emulsion mainly comprises the following components by weight: 5 to 10g of valnemulin hydrochloride, 1 to 5g of emulsifier, 20 to 40g of oil for injection, 5 to 15g of ethanol and the balance of water for injection. The valnemulin hydrochloride emulsion for animals has the advantages of quick in vivo distribution and good target, can reduce the medicament residue in vivo and the toxic or side effect on the animals, and also can mask the unpleasant odor of the medicament, and improve the stability of the medicament. The valnemulin hydrochloride emulsion for animals can effectively treat gram-positive bacteria and mycoplasma infection, particularly swine dysentery and porcine enzootic pneumonia, and can reduce the using amount of the medicament and avoid medicament tolerance.
CN102166213A Composition using levalbuterol and ipratropium bromide as active ingredients The invention provides a composition using levalbuterol and ipratropium bromide as active ingredients. The levalbuterol and ipratropium bromide can both exist in a form of medicine salt or hydrate. The composition can exist in a form of inhalant, preferably inhalation solution and aerosol. The composition can be used for treating reversible bronchospasm related to airway obstruction type diseases.
US20090320148 Oxylipins from stearidonic acid and gamma-linolenic acid and methods of making and using the same Disclosed are novel oxylipins that are derived from γ-linolenic acid (GLA; 18:3n-6) and stearidonic acid (STA or SDA; 18:4n-3), and methods of making and using such oxylipins. Also disclosed is the use of such oxylipins in therapeutic and nutritional or cosmetic applications, and particularly as anti-inflammatory or anti-neurodegenerative compounds. Also disclosed are The invention novel ways of producing long chain polyunsaturated acid (LCPUF A)-rich oils and compositions that contain enhanced and effective amounts of SDA- and/or GLA-derived oxylipins.
WO2007003767A3 Novel chemical compounds and the uses thereof as a medicine The invention concerns the field of pharmacy, especially the treatment of neurodegenerative diseases. The invention specifically relates to a family of chemical compounds of formula (I) for which a neuroprotective activity has been demonstrated. The invention further relates to compositions comprising the compounds of said family, and the use of said compounds as medicines, especially for preparing of a medicine for the treatment of neurodegenerative diseases.
CN1672679A Application of externally applied phentolamine methane sulphonate prepn in treating female sexual apathy The present invention relates to new phentolamine methanesulphonate preparations. The new phentolamine methanesulphonate preparations includes effervescent vagina tablet, suppository, lotion, liniment, alcohol preparation, spray preparation, cream, ointment, emulsion, etc. and may be in slowly or controlled releasing form. The tablet contains phentolamine methanesulphonate in 10-2000 mg each. The said preparation is used in treating female sexual apathy.
US20110086904 GENERATION OF HYPERSTABLE mRNAs Provided herein is a method for enhancing the stability of a mRNA molecule. Specifically, the invention provides methods of increasing stability or augmenting expression of mRNA or its products by inserting a stability inducing motif at the 3′UTR of the molecule.
CN101554375B Pharmaceutical composition containing clopidogrel and carbazochrome sodium sulfonate The invention provides a pharmaceutical composition containing active carbazochrome sodium sulfonate and clopidogrel or the pharmacologically acceptable salt thereof. The invention aims to invent a more effective and low adverse-reaction method for curing thrombotic diseases by using the combined medication of the carbazochrome sodium sulfonate and the clopidogrel. After conscientious trail of thepatent applicant for many times, the effect of applying the carbazochrome sodium sulfonate to inhibit the thrombosis in a combined manner is discovered unexpected in the process of applying the clopidogrel to cure the thrombotic diseases, the anticoagulant effect of the clopidogrel is not abated but increased, and the very good synergistic effects are achieved after the combination of the carbazochrome sodium sulfonate and the clopidogrel, therefore, the risk of bleeding is greatly reduced when the advantages of good anticoagulant activity and fast effect of the clopidogrel during the antiplatelet aggregation are fully exerted, the risk of bleeding caused by the clopidogrel is greatly reduced and the compliance of patients is enhanced.
US6939874 Substituted pyrimidinyl derivatives and methods of use The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.
CN101559218B Composition with function of increasing bone density The invention relates to a composition with a function of increasing bone density and a preparation method thereof. Active components comprised by the composition are calcium carbonate, glucosamine hydrochloride, chondroitin sulfate, casein phosphopeptide, and soy isoflavone. The composition is prepared by reasonably and scientifically matching and combining the raw materials, and is prepared intooral preparations which are convenient to take. Experiments prove that the composition has the function of increasing the bone density.
CN101045072A Extractive of turnipia arguta leaves and its pharmaceutical use An extract of bee sage leaf for preparing the antibacterial, antiviral, antioxidizing and antinautation medicines to prevent and treat tumor, hepatitis B, thrombus and arteriosclerosis features that it contains flavone compounds and their pharmacologically acceptable salts. Its preparing process and quality control method are also disclosed.
US6946464 Methods of treating and preventing a convulsive state The invention is directed to compositions comprising, and methods of using, racemic N-desmethylzopiclone, optically pure (+)-N-desmethylzopiclone, and optically pure (−)-N-desmethylzopiclone in the treatment and prevention of diseases and conditions in mammals. The invention is further directed to novel methods of preparing N-desmethylzopiclone, optically pure (+)-N-desmethylzopiclone, and optically pure (−)-N-desmethylzopiclone.
US20090028969 Compostion for treating skin A combination comprising verbascoside and luteolin, and its use in a cosmetic or pharmaceutical composition for pigmentation modulation.
CN102988962A Composition for preventing or treating pruritus cutanea The invention discloses a composition for preventing or treating pruritus cutanea. The composition comprises the following active components: (1) hydrolyzed collagen, (2) hyaluronic acid and (3) allantoin compound, wherein the allantoin compound is allantoin and/or allantoin aluminum compound. The compound disclosed by the invention can be used for effectively preventing or treating the pruritus cutanea, and particularly shows a good effect on treating senile pruritus.
EP2776424A1 Substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with an n-cyclic group as vanilloid receptor ligands The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with an N-cyclic group as vanilloid receptor ligands formula (S) to pharmaceutical compositions containing these compounds of the general formula (S) and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
CN101712642A 5 site-sodium thiosulfate substituted elsinochrome derivative and preparation method and application thereof The invention discloses a 5 site-sodium thiosulfate substituted elsinochrome A derivative and a preparation method and application thereof. In the preparation method, elsinochrome, sodium thiosulfate and a solvent are uniformly mixed away from light till pH value is 10-14; after the reaction is finished, the product is obtained. The derivative has the solubility of 5.1mg/mL in a buffer solution or physiological saline water and meets the requirement on safe transmission in intravenous injection administration and blood; and the preponderant lipotropism (the lipid-water allotting coefficient is about 7) of the derivative is maintained on the premise. A biological experiment indicates that the killing rate of the derivative on the human lung cancer cell (A549) is equivalent to 60 percent of the matrix elsinochrome; by the superhigh photodynamic activity of the elsinochrome, the photodynamic activity of the derivative is sufficient for meeting the clinical requirement. In conclusion, the derivative can be directly used for a clinical photodynamic medicament of intravenous injection without further preparation.
CN103524519A Camptothecin prodrug monomer and polymeric prodrug amphipathic molecules thereof as well as preparation method and application of camptothecin prodrug monomer and polymeric prodrug amphipathic molecules The invention relates to a reduced response camptothecin prodrug monomer as shown in a formula I, reduced response camptothecin polymeric prodrug amphipathic molecules of the reduced response camptothecin prodrug monomer, and a preparation method and application of the reduced response camptothecin prodrug monomer and the reduced response camptothecin polymeric prodrug amphipathic molecules. In the formula I, each i is 2 or 3 independently, each X is O or NH independently, and R is H, CH3 or CH2CH3. According to the preparation method, raw materials including camptothecin, triphosgene and the like are used for modifying 20 bits of hydroxyls of camptothecin to prepare a camptothecin prodrug monomer containing disulfide bonds, then the camptothecin prodrug monomer is subjected to high-conversion-rate polymerization by using active free radical polymerization method to obtain an amphiphilic polymer which contains a camptothecin drug repetitive unit and has an extremely high drug loading capacity (more than 50wt%), and in a tumor cell reducing environment, a side chain disulfide bond is broken to perform molecular rearrangement and release camptothecin prodrug molecules, so that the amphiphilic polymer has characteristics of a reduced response controlled-release raw drug. The polymeric prodrug amphipathic molecules improve the water solubility and stability of the drug and have a controlled release characteristic.
CN102940617A Desloratadine oral dispersible film The invention relates to a desloratadine oral dispersible film which comprises desloratadine, biologically-acceptable water-soluble polymers, plasticizers, purified water and the like, can be dispersed or dissolved quickly in the oral cavity, and is used for treating allergic rhinitis, allergic rhinitis and asthma syndrome, allergic nasal conjunctivitis, allergic dermatitis, allergic asthma and the like. The desloratadine oral dispersible film is free of irritation, convenient to take and carry, fast in effect, good in taste and particularly suitable for being used by the olds and children.
CN102557885A Novel diphenylbutadiene derivative and applications thereof in drug The invention relates to applications of a novel diphenylbutadiene derivative as an immunosuppressive agent in a drug. In the invention, the characteristics of structural properties and physiological activities and the like of natural polyphenol compounds are used for reference. The invention provides a novel diphenylbutadiene derivative, a preparation method of the new compound and applications of the novel diphenylbutadiene derivative in a drug thereof. The new compound has significant activity of an anti-inflammation skin disease. The new compound and drug combination thereof can be used for treating the diseases related with immunity and autoimmunity.
WO2011082267A8 Substituted triazolo-pyrazine compounds The present invention relates to substituted triazolo-pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrazine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
US20080306098 Pharmacokinetics of protease inhibitors and other drugs A method for modulating at least one pharmacokinetic property of a protease inhibitor upon administration to a host is provided. One administers to the host an effective amount of a bifunctional compound of less than about 5000 daltons comprising the protease inhibitor or an active derivative thereof and a pharmacokinetic modulating moiety. The pharmacokinetic modulating moiety binds to at least one intracellular protein. The bifunctional compound has at least one modulated pharmacokinetic property upon administration to the host as compared to a free drug control that comprises the protease inhibitor.
EP1089739B1 Cyclophosphamide coated tablets The invention relates to coated tablets having cyclophosphamide as active substance, containing in the core cyclophosphamide, one or more fillers, one or several dry binding agents but no pre-swollen starches, flow regulation agents and lubricants. In a preferred embodiment of the invention, the core of the film tablet contains lactose monohydrate, D-mannite or CaHPO4 as fillers, non-pre-swollen corn starch or micro fine cellulose as dry binding agents, highly dispersed silicon oxide as flow regulation agents and magnesium stearate, stearic acid, glycerin palmitostearate, polyethylene glycol, talc or glycerin monobehenate as lubricants.
WO2013054470A1 Enhancer of survival of transplanted organ Provided are: an enhancer of the survival of a transplanted organ, which can prevent the occurrence of any rejection reaction without requiring the use of any existing immunosuppressing agent; an organ preservation solution which enables the preservation of the freshness of an organ after the excision of the organ from a donor; and others. Prepared are: an enhancer of the survival of a transplanted organ, which contains 5-aminolevulinic acid (ALA) or a derivative or salt thereof and an iron compound as active ingredients; and an organ preservation solution. Preferred examples of the ALA compound include ALA, esters thereof including a methyl ester, an ethyl ester, a propyl ester, a butyl ester, a pentyl ester and the like thereof, and hydrochloric acid salts, phosphoric acid salts and sulfuric acid salts of ALA and the esters. A preferred example of the iron compound is sodium ferrous citrate.
US20110098303 Method of promoting nail growth using thyromimetic compounds The present invention provides methods and compositions for increasing the rate of nail growth in mammals, especially humans, using thyromimetic compounds.
WO2012037034A1 E-selectin antagonists Compounds, compositions and methods are provided for inhibiting in vitro and in vivo processes mediated by E-selectin binding. More specifically, particular glycomimetic compounds are described, wherein the compounds are E- selectin antagonists.
CN103012416A Method for preparing high-purity nalmefene hydrochloride The invention relates to a method for preparing high-purity nalmefene hydrochloride, and in particular relates to a method for refining the nalmefene hydrochloride. The method comprises the steps of dissolving a crude product of the nalmefene hydrochloride in right amount of hot water, cooling and separating out the high-purity nalmefene hydrochloride. The method has the following advantages: (1) through refining, the content of the nalmefene hydrochloride is up to more than 99.5%, the content of the maximum single impurity is less than 0.2%, the content of total impurities is less than 0.5% and the prepared nalmefene hydrochloride is excellent in storage stability and suitable for preparing the preparations of parenteral administration; (2) the method is simple in process, simple and convenient for operation and low in cost and suitable for industrial production; and (3) as no organic solvent is used, the damage to operating personnel and environment is avoided, the finished product has no residual organic solvent problem, the quality inspection step is simplified and the medication safety is guaranteed.
CN103561740A Combinations of alpha 7 nicotinic acetylcholine receptor activators and mGluR5 antagonists for use in dopamine induced dyskinesia in Parkinson's disease The present invention relates to novel combinations suitable for the treatment of dyskinesia associated with dopamine agonist therapy in Parkinson's disease, which comprise, as active ingredients, at least one low molecular weight nicotinic acetylcholine receptor alpha 7 activator and at least one low molecular weight metabotropic glutamate receptor 5 antagonist; to their preparation; to their use as medicaments and to medicaments comprising them.
CN1628646A Dispersed tablet of tartaric acid tolterodine tartrate The invention discloses a tolterodine tartrate dispersed tablet, which comprises tolterodine tartrate as main constituent as well as disintegrating agent, and auxiliary additive, the disintegrating agent is of dispersion tablet type commonly used, while the auxiliary addition agent is the commonly used dispersion tablet type addition agent. The dosage has the advantages of easy administration for the elderly and children, stabilized preparation, quick absorption, high biological availability, and less adverse effect. The dosage can be used as a medicament for treating frequent micturition and urinary incontinence.
CA2381819C New benzimidazolone derivatives having mixed serotonine and dopamine receptors affinity The present invention pertains to compounds of general formula (I) wherein R1, R2, R3, and R4 denote hydrogen or hydroxy with the proviso that R1, R2, R3, and R4 cannot simultaneously represent hydrogen. These compounds bind to the Serotonine and dopamine receptors and are useful in the treatment of CNS disorders.
US20060106066 Benzyl substituted (piperidin-4-yl)aminobenzamido derivatives The present invention is directed to N-benzyl substituted (piperidin-4-yl)aminobenzamido derivatives which are delta-opioid receptor modulators.
US20050009861 Inverse agonist has a functional efficacy at the alpha 1 and/or alpha 5 receptor subtypes of less than -5%, and the efficacy measured at the alpha 2 and alpha 3 receptor subtypes is greater than 5%, and is preferably a 4-oxo-1,4-tetrahydro-1,5- naphthyridine-3-carboxamide derivative This invention provides a composition for treating a cognitive disorder, which comprises an acetylcholinesterase inhibitor, and a GABAA inverse agonist selected from a compound of the formula where X and Y are as defined herein.
CN102731396A Polyamine naphthalimide compounds and application of same in preparation of pharmaceutical preparation The invention discloses polyamine naphthalimide compounds. A preparation method for the compounds comprises the following steps: (a) weighing 4-bromo-1,8-naphthalenic anhydride and N, N-dimethyl ethylene diamine according to a mole ratio of 1: 1, mixing and heating 4-bromo-1,8-naphthalenic anhydride and N, N-dimethyl ethylene diamine, reacting for 8 to 10 h and then carrying out filtering and drying; and (b) weighing and adding intermediates obtained in step (a) and alicyclic amine into a glycol monomethyl ether solution, carrying out heating and a reaction for 8 to 12 h, evaporating the glycol monomethyl ether solution under reduced pressure, dissolving obtained solids with dichloromethane, separating an obtained solution with a silica gel column and carrying out elution with an eluant. The compounds provided in the invention have obvious inhibitory effects on the liver cancer cell Bel-7402, the leukemia cell HL-60, the human lung cancer cell A549, the human uterus cancer cell Hela and the like, and antineoplastic activity of a part of the compounds is superior to that of the commonly used antineoplastic drug cisplatin. Thus, application of the compounds in preparation of antineoplastic pharmaceutical preparations is brought forward for the first time in the invention; and particularly, application of the compounds in preparation of pharmaceutical preparations used for treating liver cancers, leukemia and uterus cancers is brought forward.
WO2010026129A1 The trpvl antagonist sb-705498 for treating rhinitis The present invention relates to the use of a urea compound in the treatment of rhinitis, to aqueous pharmaceutical compositions containing said compound, in particular to compositions suitable for intranasal administration.
EP1244649B1 Cyclic amp-specific phosphodiesterase inhibitors Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
US20090005420 Inhibitors of Matrix Metallaproteinases The present invention provides novel compounds of formulas I-IX, as described herein. Also provided are compositions of compounds of formulas I-IX, methods of making compounds of formulas I-IX, and methods of using compounds of formulas I-IX. The compounds of the invention can be used to inhibit matrix metalloproteinases, and are useful to treat conditions and diseases associated therewith.
US20050070577 Compositions containing a serotonin selective reuptake inhibitor and a 5-HT2A receptor antagonist Novel compositions comprising a selective serotonin re-uptake inhibitor (SSRI), particularly sertraline, and a selective inhibitor for the binding of serotonin at the 5HT2A site. The invention relates to the use of such compositions for treating or preventing mood disorders including depression and anxiety disorders.
CN101862419B Externally applied medicament for treating closed bone injuries The invention discloses an externally applied medicament for treating closed bone injuries. The externally applied medicament is characterized by consisting of the following raw materials by weight: 5 to 20g of Himalayan teasel root, 5 to 20g of fortune's drynaria rhizome, 5 to 20g of acanthopanax bark, 5 to 13g of notoginseng root, 5 to 13g of rhubarb, 3 to 9g of cassia twig, 3 to 6g of safflower, 3 to 6g of dragon's blood, 3 to 6g of frankincense, 3 to 6g of myrrh, 0.5 to 1g of borneol, and 0.05 to 0.2g of musk. The externally applied medicament has the effects of reducing swelling, alleviating pains, activating blood circulation, dissipating blood stasis, promoting bone marrow to produce platelet, dilating blood vessels, activating blood circulation, quickening callus healing and restoring bone tissues. Proved by hundreds of cases of clinical treatment practice for years, the externally applied medicament has a perfect effect of treating closed bone injuries such as various sprain,fracture, spinal injury and the like; and a treatment course for a patient suffered from minor injuries usually is only about twenty day, the treatment course for a patient suffered from serious injuries is only about forty days, and the cure rate reaches over 95 percent.
WO2014055047A1 Combination of idebenone and donezepil The present invention is related to pharmaceutical compositions comprising idebenone and donepezil for use in symptomatic treatment of cerebral arteriosclerosis, symptoms following stroke and cerebral hemorrhage, age-associated cognitive decline, chronic cerebrovascular disease, multi-infarct dementia and mild and moderate Alzheimer's type dementia.
US20100178322 Adhesive preparation and patch preparation An adhesive preparation comprising an adhesive preparation main body comprising a support and an adhesive layer laminated on at least one surface of the support, and a release liner formed on a surface on the side opposite from the support side of the adhesive layer of the adhesive preparation main body, wherein the adhesive preparation main body has a flat plane area of 1.5-15 cm2, and a ratio of a flat plane area of the release liner to that of the adhesive preparation main body ([flat plane area (cm2) of release liner]/[flat plane area (cm2) of adhesive preparation main body]) is 1.1-7, and the release liner has a separating line. Using the adhesive preparation of the present invention, the adhesive preparation main body can be easily held with fingers and the release liner can secure a holding section having a sufficient area, the release liner can be easily detached from the adhesive preparation main body without touching the adhesive surface with fingers and the adhesive preparation main body can be easily adhered to the skin without touching the adhesive surface with fingers, whereby inconveniences such as mutual adhesion of a certain part of the adhesive surface to other part, curling of the adhesive preparation main body and the like can be prevented.
CN102526031A Sumatriptan pharmaceutical composition used in nasal cavity and preparation method thereof The invention provides a sumatriptan pharmaceutical composition used in the nasal cavity, which comprises sumatriptan and corresponding excipients. The sumatriptan pharmaceutical composition disclosed by the invention has the advantages of simple formula, low cost, great efficacy for treating migraine and effects of saving cost and improving the efficacy.
WO2009155753A1 The use of inositol derivative or salts thereof in the manufacture of medicaments as glycosidase inhibitors or medicaments for treating diabetes The use of inositol derivative or salts thereof in the manufacture of medicaments as glycosidase inhibitors or medicaments for treating diabetes, wherein the structure of inositol derivative is represented below: wherein R is -O- or -NH- or; R1 is saturated alkane-CnH2n- (0≤n≤26), R2 is H, -CH3, -COOH, cyclo-alkane, phenyl or tolylene.
US20120065242 POLYMERIC NANO-PARTICLES FOR siRNA DELIVERY USING CHARGE INTERACTION AND COVALENT BONDING Disclosed is a polymer-siRNA delivery carrier in which a siRNA is combined with a polymer and the use thereof. More specifically, there is disclosed a stable in vivo polymer-siRNA delivery carrier in which a polymer and a siRNA are combined by using charge interaction and biodegradable covalent bonding at the same time and the use thereof. The polymer-siRNA delivery carrier in which a polymer and a siRNA are combined by using charge interaction and biodegradable covalent bonding at the same time has a high siRNA deliver efficiency to a target portion in vivo. Hence, according to the polymer-siRNA binder, the siRNA for treatment can be effectively delivered to a target portion such as in vivo cancer tissue, and the like even with administration of a relatively low concentration, and thus widely used for the treatment of various kinds of diseases.
US7125889 Administering mixtures of heterocyclic imines and anticoagulants such as heparin or aspirin, to reduce blood coagualtion in mammals Methods for treating cardiovascular and related diseases such as blood clots are described. The methods are directed to concurrently administering a compound such as pyridoxal-5′-phosphate, pyridoxamine, pyridoxal, or a 3-acylated pyridoxal analogue with a therapeutic cardiovascular compound.
WO2012096494A3 Agent containing b-ring-substituted flavonoid derivatives for treating arthritis The present invention relates to flavonoid derivatives expressed by the following general formula (I), to a composition containing the pharmaceutically acceptable salts thereof as an active ingredient, and to the use of the flavonoid derivatives. More particularly, the flavonoid derivatives expressed by the following general formula (I), or the pharmaceutically acceptable salts thereof, may exhibit an activity of inhibiting the decomposition of cartilage constituents, an activity of inhibiting the decomposition of ECM, and an activity of inhibiting the expression of MMP-13, and may exhibit a superior activity of inhibiting the deterioration of joints in a chronic-arthritis animal test. Therefore, the flavonoid derivatives or the pharmaceutically acceptable salts thereof may be used in a pharmaceutical composition and a functional health food that is useful for preventing and treating arthritis.
US20090186890 Pharmaceutical Formulation of Iressa Comprising a Water-Soluble Cellulose Derivative A pharmaceutical composition comprising 4-(3′-chloro-4′-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline or a pharmaceutically acceptable salt thereof (the Agent) and a water-soluble cellulose ether or an ester of a water-soluble cellulose ether. The water-soluble cellulose ether or ester of a water-soluble cellulose ether present in the composition inhibits the rate of precipitation of the Agent from solution.
CA2116980C Chimeric and/or growth-restricted flaviviruses The invention includes a chimeric virus for use in a vaccine preparation having a genome comprising nucleic acid sequenees encoding at least one structural protein from one flavivirus and nucleic acid sequences encoding nonstructural protein, from another flavivirus. The genome preferably includes mutations within the viral. genome that reduce virus virulence and in a particularly preferred embodiment these vaccines are directed to flaviviruses such as dengue virus, tick-borne encephalitis virus and Japanese encephalitis virus.
WO2013087410A1 Treatment of migraine headaches, in particular cluster headaches The invention relates to a combination of compounds and compositions for the treatment of migraine headaches and in particular for the treatment of cluster headaches.
CN101829125B Compound combined formulation for preventing and treating osteoarthrosis and preparation method thereof The invention discloses a compound combined formulation for preventing and treating osteoarthrosis and a preparation method thereof. The compound and composite formulation comprises an active component and auxiliary materials, wherein the active component is glucosamine or a combination of the glucosamine and more than one or two of other active components, i.e. chondroitin sulfuric acid, dimethyl sulfone and collagen, and the glucosamine is glucosamine sulfate or hydrochloride or phosphate or a mixture of the glucosamine sulfate, the hydrochloride and the phosphate; and the auxiliary materials include an excipient, a disintegrating agent, a lubricating agent, an adhesion agent, a stabilizing agent and a wetting agent. The invention has good treating and preventing effects on arthritis and articulate movement damage; a prepared tablet has good disintegrating property, fast dissolution and quick results and achieves the optimal proportion of the using amount of raw materials and various auxiliary materials; and in addition, the product has enhanced stability and high absorption utility ratio.
US20080051389 mimetics of the Smac peptide, used for the treatment of cancer and autoimmune disorders The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
EP1560832A1 Pyrimido 4,5-d pyrimidine derivatives with anticancer activity Disclosed are novel pyrimido compounds of the formula (I) wherein R1 to R9 are as defined in the specification, that are selective inhibitors of both KDR an FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and the use for 10 treating cancer.
US20130065866 Dentinal drug delivery composition and screening method The present invention is a dentinal drug delivery composition composed of cationic and/or neutral porous particles containing an effective amount of a therapeutic agent, a method for using the dentinal drug delivery to provide a dental treatment, and a method for identifying anti-inflammatory agents capable of diffusing through dentin.
CN101138559A Novel medicine preparations for curing psoriasis The present invention provides a novel preparation for the treatment of the psoriasis. A set of production method for Tretinoin ethyl ester capsule is obtained after the study and research of massive technique and excipient on the Tretinoin ethyl ester. The Tretinoin ethyl ester capsule with high stability and high dissolution can be obtained by the method, which can meet the requirement of the clinical application. The present invention is effective and simple with low cost, which is applicable for the industrial production.
CN101829134A New clinical application of medical composition The invention relates to new clinical application of a medical composition, in particular to the application of the composition formed from citicoline salt and inosine or adenosine in preparing medicines for treating cerebrovascular dysfunctions, craniocerebral injuries, dementia, Parkinsonism and heart diseases, wherein the unit dosage of the citicoline salt is 0.01g-2.5g, and the unit dosage of the inosine is 0.005g-2g. When in use, the medical composition can be prepared into compound preparations, including oral preparations and injection preparations for application.
CN102908326A Asparagine tablet and preparation method thereof The invention provides an asparagine tablet which comprises the following ingredients in weight ratio: every 1000 tablets comprise 250.0g of asparagine (anhydride), 14.8g of starch (internally added), 20.0g of dextrin, 3.3g of carboxymethyl starch sodium, 2.0-2.5g of magnesium stearate and starch (15% pulp). According to a novel preparation method adopted by the invention, the weight variation happening in the process of tabletting can be improved, the product rigidity can be better controlled, the phenomena such as tablet loosing, tablet cracking and the like can be avoided, and the defect rate can be reduced; and the standard range can be achieved when the asparagine tablet is disintegrated, the inherent quality of the product can be improved and optimized, and the yield can be preferably improved. The production can be continuously and stably carried out; and the step of producing wet particles by a swinging machine in the process of production can be avoided, the product quality can be guaranteed, the working hours can be reduced, the energy consumption of the single-batch production can be saved, the loss in the process of production can be reduced, and the production can be continuously and stably carried out. The method provided by the invention is simple, ensures that no new cost is added, is suitable for the large-scale industrial production, and is higher in application value.
WO2012099454A1 Curcumin compounds and their preparations thereof Accordingly, the invention discloses compounds with enhanced bioavailability for the prevention and treatment of anti-human immunodeficiency virus (HIV), anti-tuberculosis (TB), anti-Alzheimer or anti-cancer, with the following formulas: The invention also discloses the method in synthesizing these compounds wherein the steps includes mixing curcumin, isatin derivatives or ninhydrin and sarcosine or phenyl glycine in 20 mL methanol. The mixture was then refluxed with a solvent on a water bath and excess solvent was removed under vacuum. The residue subjected to flash column chromatography using petroleum ether: ethyl acetate mixture (4:1) as eluent to afford the product. The ratio for curcumin:isatin derivative/ninhydrin:sarcosine/phenyl glycine is 1:1:2 and 1:2:4.
CA2217169C Thienyl-, furyl-, pyrrolyl- and biphenylsulfonamides and derivatives thereof that modulate the activity of endothelin Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)-furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
WO2013116720A1 Combination therapy comprising tenofovir alafenamide hemifumarate and cobicistat for use in the treatment of viral infections The use of the hemifumarate form of {9-[(R)-2-[[(S)-[[(S)-l- (isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine} (tenofovir alafenamide hemifumarate) in combination with cobicistat is disclosed. In addition, the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and elvitegravir, and the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and darunavir, are disclosed.
WO2010062559A1 Substituted pyrazoloquinolines and derivatives thereof The present invention relates to substituted pyrazoloquinolines of formula I and derivatives thereof, the use of the compounds as phosphodiesterase 10 (PDElO) inhibitors for the treatment of PDElO -modulated disorders, to pharmaceutical compositions comprising the compounds, and to the use of additional substituted pyrazoloquinolines and derivatives thereof for the treatment of PDElO -modulated disorders.
CN102743332A Ornidazole and sodium chloride injection packaged by non-polyvinyl chloride (PVC) soft bag and preparation method thereof The invention provides an ornidazole and sodium chloride injection packaged by a non-polyvinyl chloride (PVC) soft bag and a preparation method thereof. The preparation method comprises the following steps of raw material weighing, concentration preparation, dilution preparation, loading and sterilization. The sterilization comprises the following steps of adjusting an initial temperature in a sterilization device to 50 to 70 DEG C, heating to a temperature of 120 to 122 DEG C, carrying out sterilization for 8 to 15 minutes, carrying out spraying by chilled water having a temperature of 0 to 30 DEG C for cooling for 5 to 15 minutes and keeping a temperature of a sterilized product in a range of 30 to 50 DEG C. The preparation method shortens high-temperature contact time of an ornidazole aqueous solution thereby reducing ornidazole degradation, wherein total sterilization time is reduced to 35 to 45 minutes so that the content of related substances obtained by ornidazole degradation is reduced to 0.64%, and thus product quality is greatly improved. The preparation method adopts a simple feeding mode, allows a low preparation temperature, realizes a small concentrated volume, has low requirements on production equipment and conditions, realizes short preparation time and can be operated by production people easily.
CN101181231B Sustained-release implantation agent of urotrotiken The invention relates to a lurtotecan sustained-release implant, which contains lurtotecan, sustained-release excipient and certain amount of sustained-release regulator, wherein, the weight percentage of lurtotecan in the sustained-release implant is 0.1 percent to 50 percent; the sustained-release excipient mainly selects one or the combination of poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co-propyl phosphate); the sustained release regulator selects one or the combination of mannitol, sorbitol, chondroitin, gelatin and albumin, which has the weight percentage of 0 to 15 percent in the sustained-release implant; the sustained-release plant is used for the preparation of drug preparations for the treatment of solid tumors. The sustained-release implant is arranged or injected at the local part of the tumor, which can not only reduce the systemic toxic reaction of lurtotecan, but can also selectively improve the drug concentration at the local part of the tumor and strengthen the treatment effects of chemotherapy drugs, radiation therapy and other non-surgical therapies. The invention can be used for the treatment of pancreatic cancer, lung cancer, liver cancer, breast cancer, brain tumor, ovarian cancer, prostate cancer, esophageal cancer, lymphoma, osteosarcoma, colorectal cancer and other solid tumors.
WO2014026997A1 2,3-benzodiazepines What are described are BET protein-inhibitory, in particular BRD4-inhibitory, 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumour disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.
EP1701947A2 4-oxo-4,5-dihydro-furan-2-carboxylic and acid derivatives and methods of treatment of metabolic-related disorders thereof The present invention relates to certain 4-oxo-4,5-dihydro-furan-2-carboxylic acid and ester derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X, and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, and the like.
US20080009453 Pharmceutical Compositions Containing Polydatin or Its Salts and Their Application The invention discloses pharmaceutical compositions containing polydatin or its pharmaceutically acceptable salts with the effect of improving microcirculation, and their application in preparing drugs which can improve microcirculation. The compositions are an non-gastrointestinal injection preparation, the preparation can be an aqueous solution which have pH 7.0-10.0 comprising 5-50% propandiol. The dosage forms of the compositions may be lyophilizing powder injection, oral form, suppository of procto-administration and other forms of administrations comprising unguent, ointment, paste film coating and the like. The compositions may be used to treat and/or prevent diseases related to microcirculation blockage. The unit form may contain 1-1000 mg polydatin or its derivatives. The invention solves the problem of using polydatin to improve microcirculation. The composition of the invention can be used in treating shock, cardiac and cerebrovascular diseases, diseases of sense organs, diabetes complication, vaculitis related to blockage of blood vessel, hemorrhoid related to circulation obstruction, skin injury and burn.
WO2007129161A3 Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor A thienopyrimidine of formula (I) and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K with selectivity for the P110α subtype, and may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour, particularly those associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
WO2011147185A1 Immunosuppressant j2 - sodium alginate microsphere, preparation method and use thereof An immunosuppressant J2 sodium alginate microsphere, its preparation method, and use are disclosed. The microsphere comprises sodium alginate as carrier and immunosuppressant J2. The micosphere is formed by encapsulating or absorbing immunosuppressant J2 into micosphere in presence of calcium ion through a high-voltage electrostatic droplets device. Said microsphere formulation has tissue-targeting, higher bioavailability and lower whole body toxicity.
WO2013083557A1 6-difluoromethyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives The invention relates to novel 6-difluoromethyl-5,6-dihydro-2H-[l,4]oxazin-3- amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
WO2007115822A1 Thienopyrimidines having mnkl /mnk2 inhibiting activity for pharmaceutical compositions The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
CN101703511A Compound tamsulosin and finasteride sustained release capsule and preparation method thereof The invention relates to compound tamsulosin and finasteride sustained release capsules and a preparation method thereof. The compound sustained release capsule is prepared by taking tamsulosin and finasteride as medical bioactive ingredients to prepare medicine-containing pellets, coating the medicine-containing pellets by coating materials to prepare sustained release pellets, and placing the sustained release pellets into hard capsule shells. The compound tamsulosin and finasteride sustained release capsules are used for treating benign prostatic hyperplasis (BPH), can be very slowly released to maintain stable plasma concentration and longer action time, and have the advantages of less toxic and side-effects and convenient application.
CN101366695A Tylenol injection and preparation method thereof The invention relates to drug injection with antipyretic and analgesic functions on human body. The antipyretic and antalgic drug injection is prepared by paracetamol (acetaminophen) as a master material and is safe, effective and large-capacity drug injection with the antipyretic and analgesic functions. The product has exact curative effect and rapid symptomatic relief, reduces secondary pollution and plays an important role in promoting the health of human being.
CN102240260B Medicament for treating colpoxerosis and preparation method thereof The invention discloses a medicament for treating colpoxerosis and a preparation method thereof. 1,000 grams of gel is prepared from the following raw materials by weight: 10 to 20 grams of Rebamipide, 5 to 8 grams of Carbomer, 4 to 5 grams of sodium hyaluronate, 200 to 500 grams of polyethylene glycol 400, 1 to 2 grams of Edetate disodium, 18 to 22 grams of polysorbate 80, 1 to 10 grams of lactic acid, 1 to 3 grams of low polylactic acid, a proper amount of sodium hydroxide and the balance of water. The preparation method comprises the following steps of: (1) taking the Rebamipide for later use; (2) adding the polyethylene glycol 400 and the polysorbate 80 into the Rebamipide in the step (1) to obtain medicinal liquid for later use; (3) adding water into the Edetate disodium for later use; (4) mixing the polyethylene glycol 400 and the low polylactic acid uniformly by adding water; (5) adding the Carbomer and the sodium hyaluronate into the step (4) to form a gel matrix for later use; and (6) adding the lactic acid into the medicinal liquid to obtain the gel preparation. After the medicament for treating colpoxerosis is used for a period of time through vaginal administration, the colpoxerosis can be cured, so that the defects of the known technique can be overcome.
CN101311270A Eucaryon expression vector capable of inducing cell immunological response and vaccine thereof The invention relates a eukaryotic expression vector, in particular to the eukaryotic expression vector which can induce cell immune response and a vaccine thereof. The technical proposal of the invention is as follows: the nucleotide sequence of the eukaryotic expression vector, pcDNA3.1/beta2M-IL15, which can induce the cell immune response, is stated as SEQ ID NO:3 does. The construction of the eukaryotic expression vector, pcDNA3.1/beta2M-IL15, which can induce the cell immune response, is as follows: (1) human beta2 microglobulin gene promoter is cloned; (2) gene fragments of human interleukin 15 is cloned; (3) the eukaryotic expression vector, pcDNA3.1/beta2M-IL15 is constructed. The vector has the advantages of being beneficial to overcoming the defects of low immunogenicity of conventional epitope DNA vaccines and being used for prevention and treatment of tumor and virus durative infection, etc.
US20070276016 Cholecystokinin (CCK2) receptor modulators; e.g. 2-(Benzo[1,2,5]thiadiazole-4sulfonylamino)-4-fluoro-N-[1-(4-fluoro-phenyl)-ethyl]-N-methyl-benzamide; pancreatic adenocarcinoma, pain, eating disorders, gastro-esophageal reflux disease, ulcers, anxiety Certain amidophenyl-sulfanylamino-benzo[1,2,5]thiadiazole compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
CN102641282A Compound erythromycin ethylsuccinate nano emulsion antibacterial agent and preparation method thereof The invention discloses a compound erythromycin ethylsuccinate nano emulsion antibacterial agent. The diameter of nano emulsion drop is 1-100nm, and the compound erythromycin ethylsuccinate nano emulsion antibacterial agent consists of the following raw materials by weight percent: 0.2%-4.0% of erythromycin ethylsuccinate, 0.03%-1.0% of trimethoprim lactate, 25.0%-38.0% of surface active agent, 2.0%-11.0% of cosurfactant, 2.5%-9.8% of oil and the balance of distilled water, wherein the sum of the weight percents of the raw materials is 100%. The compound erythromycin ethylsucciante nano emulsion antibacterial agent is mainly used for treating mycoplasma pneumonia, genitourinary system infection, pertussis, skin and soft tissue infection, respiratory tract infection caused by sensitive bacteria and the like. The nano emulsion preparation is clear and transparent liquid, the stability is good, the absorption is rapid, the medicine is released in a targeting manner, the problem of poor dissolvability in water is solved, the drug metabolism time of the nano emulsion in body is prolonged, the auxiliary dosage is reduced, and the production cost is lowered.
CN101597294B 3-aminoalkaneacylamino-rutaecarpine and 3-aminoalkaneacylamino-7,8-dehydrorutaecarpine derivative The invention discloses a 3-aminoalkaneacylamino-rutaecarpine and 3- aminoalkaneacylamino-7,8-dehydrorutaecarpine derivative and a synthetic method and an appliance thereof. As shown in experiments, the 3-aminoalkaneacylamino-rutaecarpine and 3-aminoalkaneacylamino-7,8-dehydrorutaecarpine derivative of the invention has strong inhibition perforance on acetylcholine esterase and good inhibition selectivity and the inhibition ability to acetylcholine esterase is 500 times higher than that to butyrylcholine esterase. The compound is shown to have an application prospect of being the medicines for curing Alzheimer's disease, cerebral vascular dementia, etc.
US20110229570 Orally rapidly disintegrating tablet and process for producing same Disclosed is an orally rapidly disintegrating tablet characterized in that the tablet can be produced in a conventional tablet manufacturing facility and has a satisfactory level of hardness for practical applications, and the change in properties of the tablet (i.e., decreased in hardness of the tablet, and delay of the disintegration time of the tablet in the oral cavity) are rarely caused by factors such as humidity. The orally rapidly disintegrating tablet has hardness of 40N or more, can be disintegrated in the oral cavity within 60 seconds, and is produced by compressing of a mixture of (a) an active ingredient, (b) an excipient having good water wettability, (c) a water-insoluble polymer that is well compactible and does not substantially cause a decrease in the water wettability of the excipient and (d) a disintegrating agent.
WO2005123677A1 4-carbonyl substituted 1,1,2-trimethyl-1a,4,5,5a-tetrahydro-1h-4-aza-cyclopropa'a!pentalene derivatives as agonists for the g-protein-coupled receptor s1p1/edg1 and immunosuppressive agents The invention relates to novel pyrrole compounds of the formula (I) wherein A represents -CH2CH2-, -CH=CH-, or -NH-CH2; Ar represents phenyl; mono-, di-, or tri-substituted phenyl, wherein the substituents are independently selected from halogen, lower alkyl, lower alkoxy, hydroxy-lower alkyl, hydroxy-lower alkoxy, 1-glyceryl, 2-glyceryl, cycloalkyl, mono- or di-lower alkylamino, methylenedioxy, ethylenedioxy, trifluoromethyl and trifluoromethoxy; or unsubstituted mono- or di-substituted 2-, 3- or 4-pyridyl, wherein the substituents are independently selected from lower alkoxy and hydroxy-lower alkoxy. The present invention provides novel compounds of formulae (I), (II) and (III) that are agonists for the G protein-coupled receptor S1P1/EDG1 and have a powerful and long-lasting immunosuppressive effect which is achieved by reducing the number of cirulating and infiltrating T- and B-lymphocytes, whitout affecting their maturation, memory or expansion. The reduction of circulating T-/B-lymphocytes as a result of S1P1/EDG1 agonism, possibly in combination with the observed improvement of endothelial cell layer function associated with S1P1/EDG1 activation, makes such compounds useful to treat uncontrolled inflammatory disease and to improve vascular functionality.
US20070269505 Tamper Resistant Co-Extruded Dosage Form Containing An Active Agent And An Adverse Agent And Process Of Making Same The present invention relates to co-extruded pharmaceutical compositions and dosage forms including an active agent, such as an opioid agonist, and an adverse agent, such as an opioid antagonist. Such compositions and dosage forms are useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid. The present invention also relates to methods of treating a patient with such a dosage form, as well as kits containing such a dosage form with instructions for using the dosage form to treat a patient.
WO2009079562A3 Compositions and methods for treating and preventing skeletal muscle deficiencies The present invention relates to compositions and methods for treating and preventing skeletal muscle deficiencies. In particular, the present invention provides compositions comprising poloxamers (e.g., poloxamer 188 - P188) and methods of using the same for treating and preventing skeletal muscle deficiencies and injuries (e.g., dystrophin-deficient skeletal muscle; skeletal muscle having a contraction force deficit; skeletal muscle having a Ca2+ imbalance; skeletal muscle having microtears).
WO2011047597A1 Dihydroxy benzopyranone compounds, medical compositions thereof, and their use for treating and preventing fracture and osteoporosis Dihydroxy benzopyranone compounds, medical compositions thereof, and their use for treating and preventing fracture and osteoporosis are disclosed in the application. As indicated in the experiments, the compound of formula (I) can raise the density of rat thighbone, and has no obvious influence on the weight of rat womb.
CN101928323A 23-hydroxy betulinic acid derivative with modified sites 3, 23 and 28 as well as preparation method, preparation and application thereof The invention relates to the field of medicinal chemistry, particularly to a 23-hydroxy betulinic acid derivative. The invention further discloses a preparation method of the 23-hydroxy betulinic acid derivative as well as application of the compound of 23-hydroxy betulinic acid derivative and the medicinal composition thereof in treating tumor diseases or symptoms.
EP1885699A1 Crystalline form of benzazepinium maleate derivative The present invention relates to a novel polymorphic form of 7-[4-(4-chlorobenzyloxy)benzenesulfonyl]-8-methoxy-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepinium maleate and a pharmaceutically acceptable solvate thereof, pharmaceutical formulation, process for its preparation and its use in medicine, in particular its use as an antipsychotic agent.
WO2011090885A3 Enhanced anti-microbial pdt Present invention provides enhanced methods and improved devices to eliminate, reduce, destroy and/or inhibit undesired body fluid species, such as pathogen microbes and deteriorated or malignant cells in complex environments like blood, serum and other body fluids. In preferred embodiments, present invention provides an antimicrobial PDT treatment and devices that effectively inactivates, reduces and/or destroys both Gram (-) and Gram (+) bacteria in complex body fluids. Preferred device embodiments comprise guiding channels and at least one electromagnetic radiation source, arranged separately or in sequence. Preferably, laser device or LED-panels are used to deliver electromagnetic radiation to activate the photosensilizer. Electromagnetic radiation is preferably delivered intermittently with pulse width based on treatment parameters. When used with preferred photosensitizer composition based on Safranin O, preferred laser radiation wavelength is in the range of 500-580nm. Additionally, present invention diminishes adverse host's inflammatory responses by neutralizing the biological activity of pathogenic microorganism fragments and reducing and/or removing pathogenic microorganism fragments responsible for it.
US20100240769 Olive waste recovery The present invention relates to a process for isolating soluble dietary fibers and valuable polyphenols from olive mill wastewater, wherein the olive mill wastewater is defatted by removing the fat by centrifugation and concentrated by removing the water content. The defatted and dehydrated mixture is extracted using ethanol and an organic acid and the dietary fibers are separated from the polyphenols by precipitation of the dietary fibers in ethanol. This alcoholic residual is rich in polyphenols, known as anti-oxidants can be used as a healthy and tasty additive to drinks. The soluble dietary fibers are further separated from the insoluble dietary fibers by redissolving the precipitated dietary fibers into water whereby the insoluble dietary fibers precipitate leaving the soluble dietary fibers in solution. The soluble fibres from OMW can be used as an additive and/or a fat replacer in other food items.
WO2006067498A1 Eicosapentaenoic acid for the treatment of cancer Eicosapentaenoic acid (EPA) in free acid form having a purity of about 99 per cent was administered to patients with a history of colorectal polyps for three months. It was found that crypt cell proliferation was significantly reduced, and apoptosis significantly increased, in the colonic mucosa of the treatment group. No such significant changes were seen in the non-treatment group.
CN1775219A Medicinal formulation for preventing and treating ischemic vascular disease, and its preparing method and use The present invention discloses a cornus fruit extract and its preparation method, also discloses medicine application of said extract. Said extract contains 25-50% of morroniside and 25-40% of loganin. Said invention also discloses a medicine preparation containing morroniside and loganin for curing various ischemic diseases.
WO2013147183A1 Triazinone compound and t-type calcium channel inhibitor [Problem] To provide a novel triazinone compound which has an inhibitory activity on a T-type voltage-dependent calcium channel and is useful particularly for the treatment of pain. [Solution] Provided is a novel triazinone compound represented by formula (I) (wherein each substituent is as defined in detail in the text; R1 represents a hydrogen atom, a C1-6 alkoxy group or the like; L1 and L2 independently represent a single bond, NR2 or the like; L3 represents a C1-6 alkylene group or the like; A represents a C6-14 aryl group which may be substituted, a 5- to 10-membered heteroaryl group or the like; B represents a C3-11 cycloalkylene group or the like; and D represents a C6-14 aryl group which may be substituted, a 5- to 10-membered heteroaryl group or the like), a tautomer or a pharmaceutically acceptable salt of the compound, or a solvate of the compound, the tautomer or the pharmaceutically acceptable salt.
CA2331288C Aqueous process for manufacturing paroxetine solid dispersions A process for preparing solid, amorphous paroxetine comprising: (A) mixing paroxetine free base or a pharmaceutically acceptable paroxetine salt with water and pharmaceutically acceptable polymer; and (B) drying to form a composition comprising amorphous paroxetine and polymer, eliminating the need for organic solvents common for the solvent process. The resultant amorphous solid paroxetine composition is free from the crystalline form, and yet has good handling properties, making it suitable for pharmaceutical use in the traditional tablet dosage form.
CN101270101A Method for preparing potassium sodium dehydroandroan drographolide succinate for injection and its freeze-dried injection The present invention discloses a preparation method of Yanhuning and freeze-dried powder injection. In the preparation method of the Yanhuning, Chuanhuning is dissolved in injection water with the weight of 4 to 5 times of the Chuanhuning; then 0.1 to 0.2mol/L of the sodium hydroxide solution is used for adjusting the pH value of the mixture to be 7.1 to 7.5; activated carbon is added for separating impurities; microporous membranes with 0.45 Mu m and 0.22 Mu m are orderly used for filtration; the filtrate is collected, cooled and then dried; thus the Yanhuning can be prepared. In the preparation method of the freeze-dried injection, the Yanhuning and sodium chloride are dissolved in the injection water at the temperature of 45 to 60 DEG C; after the mixture is mixed well, the activated carbon that is used by a needle and weighs 0.1 percent of the weight of the solution is used, so that the pH of the solution can be controlled between 6.4 and 6.8; the injection water is added until the weight of the solution reaches to the required amount; the solution is filtered and decarbonized; then the solution is orderly filtered by the microporous membrane of 0.22 Mu m, the microporous membrane that can block the substance of molecular weight of 10000 Dalton and the microporous membrane of 0.22 Mu m; the filtrate is collected, cooled and dried; thus the freeze-dried injection of Yanhuning can be prepared.
CN102775515A Amphiphilic chitosan derivatives, and preparation method and application thereof The invention discloses amphiphilic chitosan derivatives, and a preparation method and application thereof. The structural formula is diclosed as Formula I, wherein M represents a hydrophobic group, T represents a target ligand group, and n is 1200-4500; MCOOH is selected from at least one of deoxycholic acid, folic acid, hyaluronic acid, alanine, valine,, leucine, isoleucine, phenylalanine, tryptophane, tyrosine and proline; and TCOOH is selected from at least one of folic acid, epidermal growth factor, transferrin, nucleic acid aptamer, antibody and oligomer polypeptide. The chitosan derivatives disclosed by the invention can self-assemble into a micelle in a water solution, the hydrophobic core can be coated on the hydrophobic molecule, and the hydrophilic shell can specifically target the specific position through ligand modification. The particle size, medicine coating efficiency, drug loading efficiency and in-vivo drug release behavior of the micelle can be controlled by changing the hydrophilic group/hydrophobic group proportion. The derivatives have the advantages of mild and simple synthesis conditions, favorable biocompatibility and favorable biodegradability.
WO2013079007A1 Donepezil pamoate, preparation methode and its use The composition containing a pamoate salt of donepezil, the method of preparation and the use thereof are disclosed.
US20080233086 Expression Vectors for Treating Bacterial Infections The present invention is compositions and methods for producing anti-bacterial polypeptides, and for using those compositions and methods for treating diseases and conditions caused by a bacterial infection. More specifically, the compositions and methods include treating a gram-negative bacterium with a gram-positive host that produces a polypeptide effective against the gram-negative bacterium.
CA2504796A1 Polymorphs of pantoprazole sodium salt and process for the preparation thereof Novel crystalline forms of pantoprazole sodium salt solvate with ketone solvents, a process for the preparation thereof, the use of said forms for the purification of pantoprazol, pharmaceutical compositions therefrom and the use thereof in therapy.
US7108871 Isoflavones and saponins in defined ratios, menopause, cancer A soya extract having a content of glucoside isoflavones of at least 13% by weight and a content of 0.6 to 1.5 parts by weight of group 3 soya saponins per 1 part by weight of glucoside isoflavones. Also, pharmaceutical compositions containing this extract and methods of administering the extract to treat conditions such as pre- or post-menopausal symptoms, cancer, such as breast or prostate cancer, or alcoholism. The extracts are made by a process which includes the steps of treating ripe whole soya beans or oil-free soya flour with an aliphatic alcohol to obtain a first extract; concentrating the first extract to form a concentrated first extract; purifying the concentrated first extract by treatment with at least one aliphatic hydrocarbon; and extracting active components from the purified concentrated first extract with a water-immiscible aliphatic alcohol to obtain a second extract. Preferably, the final extract is concentrated dried to form the desired soya extract.
WO2008114143A1 Extended release formulations of macrolide antibiotic The present invention relates to an extended release formulation of macrolide antibiotic. More particularly, the present invention relates to an extended release formulation of erythromycin derivatives. The present invention also relates to a process for the preparation of extended release formulation containing erythromycin derivatives.
WO2007084473A2 The use of memantine and brimonidine to attenuate vitreoretinal vascular endothelial growth factor (vegf) protein levels in animals Reducing the VEGF level in a patient suffering from an ocular disease or condition which is characterized by elevated VEGF and/or blood retina barrier (BRB) breakdown which comprises treating said patient with an effective amount of a compound selected from the group consisting of memantine, brimonidine and mixtures thereof.
US20080260859 Dietary supplement to treat dry eye condition; fish oil triglycerides, eicosapentaenoic acid, docosahexaenoic acid, gamma-linolenic acid, zinc sulphate, vitamin E, vitamin C, vitamin B6, vitamin B12; solid, liquid, or gel; glycerol monostearate, lecithin, gelatin A composition comprises at least an omega-3 fatty acid, at least an omega-6 fatty acid, and zinc. The composition is advantageously administered to a subject suffering from a condition of dry eye. In certain embodiment, the amount of omega-3 fatty acid is much higher than that of the omega-6 fatty acid.
WO2008021338A3 Tricyclic oxazolidone derivatives useful as pr modulators Compounds of the following structure are described (I), wherein R1-R6, R16, m, V, W, X, Y, and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
US20080227792 3,4-Dihydro-1H-Isoquinoline-2-Carboxylic Acid 5-Aminopyridin-2-Yl Esters Novel compounds of formula (I), pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.
CN103012358A Compound extracted from antrodia camphorate, medical composition containing compound and application of compound The invention discloses a new compound extracted from antrodia camplhorate, a related compound shown in formula (1) and a medical composition containing the compound shown in formula (1) and a medically acceptable carrier or excipient. The invention also discloses an application of the compound shown in formula (1) to prepare a preparation used for inhibiting cancer cells. The compound extracted from the antrodia camplhorate disclosed by the invention has the function of inhibiting growth activity of tumour cells of a human body, so that a tumour can be effectively prevented and treated. Formula (1) is described in the specification.
EP1399156B1 Alkylidene pirazolidinedione derivatives and their use for treating diabetes and obesity The present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) for the treatment and/or prevention of diabetes type I and/or II, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity and polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel alkylidene pyrazolidinedione derivatives. (I) R1 and R2 represent independently from each other an unsubstituted or substituted aryl or heteroaryl.
CN102898499A Benzopyran triterpene, medicinal composition thereof and preparation method and application of benzopyran triterpene The invention provides a novel benzopyran triterpene compound, a preparation method of the novel benzopyran triterpene compound, a medicinal composition taking the compound as an active ingredient, and applications of the compound and the medicinal composition to preparation of anti-tumor medicaments, anti-bacterial agents, antifeedants and nematicides.
EP2643005A1 Composition comprising hydrolysed proteins and oligosaccharides for treating skin diseases The invention discloses a composition comprising at least one N-acetyl lactosamine, at least one sialylated oligosaccharide and at least one fucosylated oligosaccharide, and a hydrolysate comprising partially and/or extensively hydrolysed proteins, for use in the prevention and/or treatment of skin conditions and skin diseases. Preferably said composition is a starter infant formula. Said skin disease is in particular atopic dermatitis.
CN103058976A Quercetin alpha crystal-form substance, preparation method thereof, pharmaceutical composition thereof and purpose thereof The invention discloses an alpha crystal-form substance of a quercetin compound with a chemical name: 3,5,7,3',4'-pentahydroxyflavone, a preparation method thereof, a pharmaceutical composition containing the quercetin alpha crystal form and mixed crystal forms of the alpha crystal form, and an application of the quercetin crystal form substances as effective medicament components in preparing medicaments for treating neurological diseases, cardiovascular system diseases, immune system disease and anti-inflammatory diseases.
WO2007075825A2 Lipophilic anticancer drug compounds Lipophilic di (anticancer drug) compounds of formula (I): D - A - R1 - A1 - D, compositions that include the compounds, and methods for treating a cell proliferative disease using the compounds .
CN1626106A Medication for preventing and treating diseases of pigs A veterinary medicine for preventing and treating the frequently encountered diseases of pig, such as metritis, mammitis, acyesis, sterility, dysentery, epidemic enteritis, paratyphoid, asthma, etc is prepared from 15 raw materials including florfenicol, amoxicillin, lucomycin, doxycycline, etc.
CN101496795B Technique for preparing biodegradable composite controlled release membrane of medicament The present invention provides a biodegradation compound medicine controlled release film and a process for preparing the same. The film is designed aiming at solving the technical problems that the prior dressing film has relatively poor mechanical strength to different extents, is hard to keep the wound surface wet, has unobvious treating effect on the wound surface, high price and certain antigenicity, and is uneasy to apply in wide range, and the like. The release film is prepared from the following components in percentage by weight: 0 to 35 percent of chitosan, 50 to 100 percent of PLA or PLGA and 0.1 to 25 percent of anti-inflammation and sterilization medicines. The preparation process is realized by the following steps that: firstly, the chitosan and the PLA or PLGA are dissolved in a cosolvent, namely trifluoroacetic acid and prepared into an even solution, and the even solution is added with medicine components, subjected to ultrasonic oscillation to fully dissolve and disperse the medicines, and then subjected to flow casting and film forming. The film has the characteristics of good film forming property, medium mechanical strength, good blood stopping effect, medium degrading speed, the maintaining of the wetness on the wound surface, obvious anti-inflammation and sterilization effects, simple preparation process and low cost, and can be widely used for the treatment of the wound surfaces of burning and hurting and the recovering treatment of operation wound.
CN103709170A Medicinal crude drug for reducing blood sugar The invention relates to a medicinal crude drug for reducing blood sugar. The active component of the crude drug is a compound shown as a formula I, or acid addition salt of the compound such as phosphate or solvate of the compound such as aquo-complex, and the crude drug also comprises optional impurity D and impurity N, wherein, relative to the free alkali of the compound of formula I, the content of the impurity D is less than 0.5%, and the content of the impurity N is less than 0.5%. The invention also relates to a medicine composition prepared by the crude drug, a preparation method for the crude drug and the application of the crude drug. The crude drug can be used for preventing or curing diabetes mellitus II, hyperglycemia, insulin resistance, obesity and high blood pressure as well as complication of the diabetes mellitus II, hyperglycemia, insulin resistance, obesity and high blood pressure.
CN103387582A Coumarin natural product, and preparation method and application thereof The invention belongs to the pharmaceutical field, relates to an application of a furocoumarin compound in inhibiting a resistant staphylococcus aureus, and a preparation method for the furocoumarin compound, and particularly relates to an application of the furocoumarin compound in preparing a TetK tetracycline-containing outer pump protein and a methicillin-resistant staphylococcus epidermidis staphylococcus aureus drug. The pharmacological activity results of the compound show that the furocoumarin compound presents specific inhibition activity for the TetK tetracycline-containing outer pump protein drug-resistant staphylococcus aureus strain XU212 and mecA gene-containing methicillin-resistant staphylococcus epidermidis staphylococcus aureus strain EMRSA-16; and the inhibition activity is obviously stronger than that of contrast drugs of tetracycline and oxacillin. The drug provided by the invention can be used for preparing a plurality of preparations such as antibiotic injections, externally-applied drug preparations, etc.
CN101371847B Use of pseudo ginsengenin in preparing medicament for resisting platelet aggregation The invention relates to an application of simulated ginsengenin in the preparation of platelet aggregation inhibitor. The invention also provides a medicinal composition that contains ginsengenin or ginsengenin salts and is used for treating and preventing platelet aggregation.
CN102805867A Application of transcription factor NFATC3 as drug target in reversing multidrug resistance of tumor The invention provides a new use of a transcription factor NFATC3 (nuclear factor of activated T cell 3), namely an application of the transcription factor NFATC3 as a drug target in reversing multidrug resistance of a tumor. A drug is an NFATC3 inhibitor which comprises tacrolimus, cyclosporin A or VIVIT; and the multidrug resistance of the tumor is mediated by P-gp. The important points of the application are that a close tie between the transcription factor NFATC3 and the multidrug resistance is found, and the NFATC3 inhibitor has an obvious reversing effect on the multidrug resistance of tumor cells, and has little toxic or side effect; and therefore, the invention provides a new target for the design of a new drug which resists the multidrug resistance, of the tumor and a new clue for reversing the multidrug resistance of the tumor.
CA2697551C Piperidine derivatives as modulators of gpr119 activity The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. Compounds of this invention are of general Formula I as follows. (see formula I)
CN1739565A Dietotheraupeutic nutrient for preventing and treating secondary diabetes and its prepn process The dietotherapeutic nutrient for preventing and treating secondary diabetes consists of purine nucleotide, compound vitamin, compound trace elements, compound mineral matter, essential fatty acid oil and proper amount of edible cellulose as stuffing and hypoglycemic. The dietotherapeutic nutrient is used as main material or additive for food products and medicines for preventing and treating diabetes through balancing insulin and hyperglycemic hormone, repairing the functions of pancreatic island and kidney, preventing and treating complication and restoring normal synthesis and metabolism. The present invention has c-GMP, trace elements, etc. to regulate second messenger c-AMP amount, lift, activity and release time of hyperglycemic hormone, calcium carbonate to buffer and neutralize flavone and other acid matter and acid poisoning, potassium citrate to replenish potassium and to maintain acid-alkali and electrolyte balance. The dietotherapeutic nutrient has no toxic side effect and dependence.
WO2013189905A1 Pyrrolopyrazone inhibitors of tankyrase There are provided compounds of the formula (I), wherein R1 and R2 are as described herein. The compounds are useful as inhibitors of tankyrase in the treatment of cancer.
EP0877555B1 Use of an inhibitor of an immune system costimulation event for the preparation of a medicament inhibiting the immune system destruction of transplanted viable non-embryonic cells This invention provides a method of inhibiting viable cells transplanted into a subject from being destroyed by the subject's immune system which comprises: a) containing the viable cells, or tissue comprising the viable cells, prior to transplantation within a device comprising a semipermeable membrane; and b) treating the subject with a substance which inhibits an immune system costimulation event in an amount effective to inhibit the subject's immune sytem from responding to said contained cells or tissue. In one embodiment, the substance which inhibits an immune system costimulation event is CTLA4. Also provided by this invention is a method of treating diabetes in a subject which comprises: a) containing viable insulin-producing cells, or tissue comprising such cells, within a device comprising a semipermeable membrane; b) transplanting an effective amount of such contained viable insulin-producing cells into the subject; and c) treating the subject with an effective amount of a substance which inhibits an immune system costimulation event.
US8795634 Absorption of therapeutic agents across mucosal membranes or the skin Absorption of a therapeutic agent across a mucosal membrane or the skin can be enhanced using an absorption enhancer comprising a hydroxy fatty acid ester of polyethylene glycol.
CN103462927A Preparation method for daytime-taken softgel for treating cold The invention discloses a preparation method for a daytime-taken softgel for treating a cold. The preparation method comprises the following steps: A, preparation of a gelatin liquor: dissolving plasticizer in water, adding into a gelatin melting tank, adding gelatin, stirring to dissolve, adding coloring agent into water, stirring uniformly to obtain a pigment solution, adding the pigment solution into an obtained gelatin solution, stirring and vacuumizing to exhaust air bubbles, so as to obtain the gelatin liquor; B, preparation of contents: adding mixed polyethylene glycol and polyhydric alcohol into polyvidone, stirring to dissolve, adding acetaminophen, stirring to obtain a suspension, adding into a proportioning tank, vacuumizing, filling with inert gas, heating to dissolve, cooling, adding dextromethorphan hydrobromide and phenylephrine hydrochloride, vacuumizing, and keeping the temperature to dissolve, so as to obtain a content solution; C preparation of the softgel: adding the gelatin liquor and the content solution into a pelleting machine respectively, pelleting, drying, pellet plastering and packaging. The invention aims to provide the preparation method for the daytime-taken softgel which is used for treating the cold, and is simple in process, convenient to manufacture and good in product stability.
WO2009061889A3 Grape polyphenolics for platelet and bacterial control Special extracts of grape berries and Goji berries can be prepared by exposing fruit juices or preparations to an insoluble binding resin which is then extracted with soluble polyvinylpyrollidone. Grape and Goji extracts made in this way can be used to inhibit or control platelet aggregation. Grape extract has exceptional antibacterial properties and can be used to control oral bacteria and to control MRSA (Methicillin-resistant Staphylococcus aureus). The combination of control of platelet aggregation and antibacterial properties exhibited by the grape-extract allows it to be used to significantly extend the life of isolated platelets. When added to solutions of isolated platelets, the grape extract prevents bacterial growth and prevents deterioration of the platelets through activation. This treatment extends the usable life of platelet concentrates to at least ten days. In addition, polyphenols can be used as a medicament for modulation of platelet activity in vitro.
CN102731464A Sesquiterpene lactone compound, its preparation methods and application Belonging to the field of medical technologies, the invention specifically relates to a sesquiterpene lactone compound, its preparation methods and application of the compound in preparation of anti-tumor substances. The structure of the sesquiterpene lactone compound is shown as the following.
CN101773477B Ceftiofur lung targeting microsphere used for beasts and birds and preparation method thereof The invention provides a ceftiofur lung targeting microsphere used for beasts and birds and a preparation method thereof, which can solve the problems of waste of a large amount of medicine, indistinctive curative effect, medicine toxic and side effect enhancement and high possibility of generating medicine resistance caused by few reached targeting parts in the prior art. The invention has the technical scheme that ceftiofur is used as raw materials, gelatin is used as carriers, and the weight ratio of the ceftiofur to the gelatin is 1/0.5 to 20. The invention also provides a preparation method of the lung targeting microsphere. Both the medicine carrying rate and the encapsulation rate of the microsphere are high, the encapsulation rate can reach more than 60 percent, and more than 94 percent of sorted microspheres have the grain diameter between 7 and 30 mum, so the requirement of the lung targeting microsphere on the grain diameter is met, the tissue selectivity of the medicine isimproved, the effect of lung targeting is reached, the concentration of the medicine in other tissues is lowered, the toxic and side effect is reduced, and thus, pulmonary infection of animals can betreated at high efficiency.
CA2591867C Cooling topical patch preparation Topical patch preparations that contain an odorless physiological cooling agent, and methods for using the same are provided. The subject topical patch preparations are made up of an adhesive gel composition that is present on a support, where the adhesive gel composition includes the odorless physiological cooling agent, a water-soluble polymer gel, water and a water holding agent. In using the subject topical patch preparations, the topical patch preparations are applied to a skin surface of a subject and maintained at the site of application for a period of time sufficient for an effective amount of the an odorless physiological cooling agent to be administered to the subject. The subject invention finds use in a variety of applications.
CN103142607A Preparation method of tegafur gimeracil oteracil potassium capsule The invention provides a preparation method of a tegafur gimeracil oteracil potassium capsule. The preparation method comprises the following steps of: dispersing tegafur, gimeracil and potassium oxonate in a hydrophilic material aqueous solution; grinding by utilizing a ball mill; then spray-drying; evenly mixing the spray-dried material with a lubricant; and filling the mixture into a capsule.
US7329651 Cannabimimetic ligands Disclosed are heterocyclic compounds and methods for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoids. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual and to treat a condition in an animal or individual.
US20090306001 Novel amphiphilic derivatives of alpha-c-phenyl-n-tert-butylnitrone Compounds derived from α-C-phenyl-N-tert-butylnitrone, a process for the preparation thereof and use thereof for the preparation of medicaments for use in preventing or treating oxidative stress-related diseases.
US20100004309 Dietary Compositions and Methods for Protection Against Chemotherapy, Radiotherapy, Oxidative Stress, and Aging The present invention relates to dietary compositions comprising reduced level of methionine, tryptophan, all amino acids, or protein, dietary compositions comprising glycerol as a substitute for monosaccharides, disaccharides, and polysaccharides, and hypocaloric or calorie free diets with reduced level of energy, carbohydrates, or protein. Also disclosed are methods of using these compositions and diets, as well as fasting, to protect subjects against chemotherapy, radiotherapy, oxidative stress, or aging.
US20110027183 Hydrophobic Modified Pres-Derived Peptides of Hepatitis B Virus (HBV) and Their Use as Vehicles for the Specific Delivery of Compounds to the Liver The present invention relates to hydrophobic modified preS-derived peptides of hepatitis B virus (HBV) which are versatile vehicles for the specific delivery of compounds to the liver, preferably to hepatocytes, in vitro as well as in vivo. Any kind of compound, but in particular drugs, such as interferons, viral reverse transcriptase inhibitors or core assembly inhibitors, and/or labels can be specifically targeted to the liver and so be enriched in the liver. This liver targeting can further be used for the targeted diagnosis, prevention and/or treatment of liver diseases or disorders, such as hepatitis, malaria, hepatocellular carcinoma (HCC), as well as for the prevention of HAV, HBV, HCV and/or HDV infection. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified preS-derived peptide(s) and the compound(s) to be specifically delivered to the liver. The present invention furthermore relates to a method for the combined treatment of a liver disease and the prevention of HAV, HBV, HCV and/or HDV infection. The present invention relates also to the use of the preS-derived peptides in gene therapy and the delivery of immunogenic epitopes for hepatocyte-mediated antigen presentation to activate liver-directed immunological responses.
CA2856722A1 Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.
CN103041115A Composition for treating leukemia A composition for treating leukemia comprises the following raw materials in terms of weight: 10 g radix trichosanthis, 10 g raw oyster shells, 10 g houttuynia cordata, 10 g mineral pills, 10 g centipedes, 10 g common camptotheca fruits, 10 g rabdosia longituba, 10 g leeches, 10 g green Chinese onions, 10 g rhizoma corydalis, 10 g magnetite, 10 g Chinese date, 10 g borneol, 10 g ginseng, 10 g poria cocos, 10 g pinellia ternata, 10 g toad, 10 g Euphorbia pekinensis, 10 g nux vomica, 10 g radix aconiti agrestis, 10 g corydalis amabilis, 10 g semen momordicae, 10 g Saussurea involucrata, 10 g pearl powder, 10 g pillbugs and 10 g long-noded pit viper. The composition provided by the invention is effective and has no toxic and side effect.
CA2846046A1 Bicyclic heteroaromatic compounds Compounds of formula I, wherein X1, X2, X3, X4, X5, R1 , R2, R3, R4, R5 and R6 have the meanings indicated in claim 1, are kinase inhibitors and can be used, amongst other things for treating tumors.
WO2008078785A1 Klf5 suppressor and method for selecting active ingredient of the medicament It is intended to discover a new medicament capable of suppressing the action of KLF5 which is present as a transcription factor and is associated with the onset, progression or the like of various diseases, and to provide new means for prevention or treatment of the diseases. More specifically, it was found that the abundance of the KLF5 was suppressed by a proteolytic action through a nuclear receptor, and that the above object can be achieved by providing a medicament containing a substance binding to a nuclear receptor which has an action of suppressing the amount of KLF5 protein as an active ingredient. Further, the invention provides a method for selecting the active ingredient of the medicament suitable for the mechanism of degradation of the KLF5.
CN103622929A Acotiamide hydrochloride sustained release tablet and preparation method thereof The invention discloses an acotiamide hydrochloride sustained release tablet and a preparation method thereof. The sustained release tablet, in unit dose package, comprises 150mg of acotiamide hydrochloride trihydrate, 200 to 300mg of sustained-release material, 300 to 400mg of stabilizer, adhesive, lubricant and coating material. The sustained release tablet has 12-hour sustained release effect and good chemical stability. The releasing rate of the sustained release tablet is good in repeatability from laboratory to mass production stages, and is basically unchanged through 6 month stability inspection.
WO2012076555A1 Autophagy enhancing compounds, peptides and peptidomimetic compounds for use in the treatment of neuronal diseases The present invention relates to autophagy enhancing compounds or a pharmaceutical compositions comprising these compounds for use in the treatment of neuronal diseases, in particular acute focal brain lesions.
CN103720687A Application of dicoumarol to preparation of drug for treating or preventing influenza virus infection The invention discloses an application of dicoumarol to the preparation of a drug for treating or preventing influenza virus infection. Firstly, the toxicity effect of an MDCK (Madin Darby Canine Kidney) cell on the dicoumarol is detected, and the result shows that the maximum non-toxic consistency of the dicoumarol is 50.0 mum; secondly, the antivirus activity of the MDCK cell is detected within a completely non-toxic consistency range, and the result shows that the small molecular compound has remarkable antivirus activity, and the antiviral effect has a dosage dependence effect; finally, the antiviral activity of the dicoumarol for resisting different types and subtypes of influenza viruses is detected, and the result shows that the dicoumarol can resist the copy of a detected influenza virus strain in a dosage independence manner and the influenza virus resistance activity is broad-spectrum. Therefore, the dicoumarol disclosed by the invention is a novel broad-spectrum influenza virus resistant drug, and can be applied to the preparation of drugs for preventing or treating the influenza virus infection.
CA2317721C Novel steroid-activated nuclear receptors and uses therefor A novel nuclear receptor, termed the steroid and xenobiotic receptor (SXR), a broad-specificity sensing receptor that is a novel branch of the nuclear receptor superfamily, has been discovered. SXR forms a heterodimer with RXR that can bind to and induce transcription from response elements present in steroid-inducible cytochrome P450 genes in response to hundreds of natural and synthetic compounds with biological activity, including therapeutic steroids as well as dietary steroids and lipids. Instead of hundreds of receptors, one for each inducing compound, the invention SXR receptors monitor aggregate levels of inducers to trigger production of metabolizing enzymes in a coordinated metabolic pathway. Agonists and antagonists of SXR are administered to subjects to achieve a variety of therapeutic goals dependent upon modulating metabolism of one or more endogenous steroids or xenobiotics to establish homeostasis. An assay is provided for identifying steroid drugs that are likely to cause drug interaction if administered to a subject in therapeutic amounts.
CN101049336A New composition of medication for anti cancer An anticancer medical composition for treating cancers, leukemia, hepatitis, hepatocirrhosis, etc is proportionally prepared from gynostemma pentaphyllum or its extract, cordyceps or its extract, cantharidin or its derivative or its analog, and/or toad venom or its extract. It can be used the relative medicine by mixing it with the pharmacologically acceptable auxiliaries.
WO2008082250A1 Improved process for the preparation of non-crystalline atorvastatin calcium The present invention relates to an improved process for the preparation of non-crystalline atorvastatin calcium salt. The preparation process according to the present invention first comprises a step of completely dissolving atorvastatin calcium, thereby converting any known crystalline atorvastatin calcium to the non-crystalline form. Accordingly, the process is very useful to convert the crystalline atorvastatin calcium to the non-crystalline form.
CN103565820A Bacterial cellulose preparation for prevention and treatment of chronic obstructive pulmonary disease The invention belongs to the technical field of biology, and particularly relates to a bacterial cellulose preparation for prevention and treatment of a chronic obstructive pulmonary disease. The bacterial cellulose preparation adopts the following technical scheme: first preparing bacterial cellulose, then pulping the bacterial cellulose, mixing the pulped bacterial cellulose with mature vinegar, and performing high-pressure homogeneous emulsion and sterilization to obtain the bacterial cellulose preparation that is used for prevention and treatment of the chronic obstructive pulmonary disease. The bacterial cellulose has a function similar to that of human lung tissue cilia, and can effectively absorb and discharge toxic substances, and the mature vinegar component in the bacterial cellulose preparation can play effects of effective treatment of pulmonary inflammation, softening mineralized lung tissues in a lung, and improvement of lung functions, so that the chronic obstructive pulmonary disease can be prevented and treated by spraying of the bacterial cellulose preparation.
WO2008076806A3 Compositions and methods to potentiate colistin activity A pharmaceutical composition comprising an antimicrobial agent and an enhancer of an antimicrobial agent, wherein the enhancer of an antimicrobial agent is an inhibitor of gene, that by inactivating the gene product potentiates the effectiveness of the antimicrobial agent. In some embodiments, the pharmaceutical composition further comprises a pharmaceutically acceptable carrier. In some embodiments, the antimicrobial agent is an antimicrobial peptide such as a polymyxin, for example but not limited to colistin. In some embodiments of the present invention provides methods to treat and/or prevent infection of a subject with a microorganism by administering a pharmaceutical composition comprising an antimicrobial agent and an enhancer of an antimicrobial agent. In some embodiments, the present invention provides methods to inhibit growth of a microorganism by administering a pharmaceutical composition comprising an antimicrobial agent and an enhancer of an antimicrobial agent.
WO2012049222A3 Novel omega-3 and omega-6 fatty acid compositions and uses thereof A composition for use in preventing and/or treating and/or reducing organic, including symptomatic, mental disorders, comprising: a) Docosahexaenoic acid (DHA) and/or the pharmaceutically acceptable derivatives and/or precursors thereof; b) Eicosapentaenoic acid (EPA) and/or the pharmaceutically acceptable derivatives and/or precursors thereof; c) γ-linolenic acid (GLA) and/or the pharmaceutically acceptable derivatives and/or precursors thereof; and at least one vitamin selected from vitamin B6, folic acid, vitamin B12, vitamin E, and/or vitamin D, at least one mineral which is selenium and/or zinc, optionally other vitamins, and optionally a polyphenolic plant extract with antioxidant properties.
US6893858 Human kcnq5 potassium channel, methods and compositions thereof An isolated polynucleotide encoding a novel potassium channel polypeptide, KCNQ5, that is expressed primarily in brain and skeletal muscle is described. The new polypeptide has been cloned and isolated from a human brain cDNA library and is a member the KCNQ family of potassium channels. The provided human KCNQ5 nucleic acid sequence and encoded polypeptide can be employed for diagnostic, screening and therapeutic uses. Moreover, the hKCNQ5 polypeptide can be used to assay for KCNQ5 potassium channel modulators, which can be utilized in the treatment of neurological, neurophysiological, neuropsychological and neuroaffective diseases, conditions and disorders, including, but not limited to, acute and chronic pain, migraine, acute stroke, dementia, vascular dementia, trauma, epilepsy, amyelotrophic lateral sclerosis (ALS), multiple sclerosis (MS), Parkinson's Disease, learning and cognitive disorders, and neurophysiological disorders including anxiety disorders, depression, bipolar disorders, sleep disorders, addiction, and eating disorders.
WO2009104045A1 Ophthalmic gemifloxacin compositions for the treatment of ocular infections New compositions for ophthalmic use are described, comprising gemifloxacin, a polymer component and optionally also buffer, isotonizing and preserving agents. The compositions reveal- a marked affinity for specific ocular compartments, enabling an effective antibiotic treatment to be administered to different districts of the eye with an ample safety margin.
WO2008059261A1 Clotrimazol for treating staphylococcal infections There is described clotrimazole, l-[(2-chlorophenyl) diphenylmethyl]-lH-imidazole (C22H17ClN2); and derivatives thereof, for the treatment of an infection caused by or contributed to a methicillin resistant Staphylococcus species. There is also described a method of treating a patient suffering from an infection caused by or contributed to a methicillin resistant Staphylococcus species, said method comprising the step of administering an effective amount of clotrimazole, and derivatives thereof.
EP2510948A1 T cell activation inhibitor, pharmaceutical composition containing same, and screening method for t cell activation inhibiting substance Provided is a T cell activation inhibitor containing an RGM inhibiting substance such as an anti-RGM neutralizing antibody and the like as an active ingredient. The T cell activation inhibitor is useful as a pharmaceutical composition for the prophylaxis or treatment of autoimmune diseases such as multiple sclerosis and the like, and other diseases caused by T cell activation. In addition, a T cell activation inhibiting substance can be screened for by contacting a test substance with RGM and selecting a test substance that lowers the activity level of RGM.
EP0873110B1 Improved hemostatic composition for treating gingival area A hemostatic dental composition for controlling oral bleeding or providing gingival tissue fluid control, which includes a hemostatic agent, a chemical agent for reducing the acidic activity of the hemostatic agent, and an aqueous base. The composition can be used to stop bleeding or control gingival tissue fluid flow without opening up the dentinal tubules in the dentin of a tooth that has been cut during dental restorative and reconstructive procedures. The chemical agent is preferably an inorganic filler or high molecular weight polyol that reduces the acidic or other chemical activity of the hemostatic agent. This allows the smear layer plugs in the dentinal tubules to remain substantially intact to occlude passage of potentially harmful contaminants into the tubules and hence into the dental pulp.
US20130028962 Triggered Cargo Release from Nanoparticle Stabilized Liposomes Control of the fusion activity of liposomes by adsorbing biocompatible nanoparticles to the outer surface of phospholipid liposomes is disclosed. The biocompatible nanoparticles effectively prevent liposomes from fusing with one another. Release of cargo from the liposome is accomplished via trigger mechanisms that include pH triggers, pore forming toxing triggers and photosensitive triggers. Dermal drug delivery to treat a variety of skin diseases such as acne vulgaris and staph infections is contemplated.
WO2014059346A1 Methods for the treatment of conditions involving dopamine through administration of piperazine compounds Disclosed embodiments are related to pharmaceutical compositions and methods for preventing or treating conditions involving dopamine, such as Parkinson's disease, comprising administering to a mammal in need thereof, an effective amount of a vanoxerine metabolite.
US20080269187 Applying propylene glycol to ear with antibiotic, viricides, fungicide, antiinflammatory agents Methods for treating and preventing middle ear infections by transmembrane administration of medicament-containing transmembrane carrier compositions comprising a chemical penetration enhancer, such as propylene glycol. The compositions are applied to the ear so as to contact the outer surface of an intact tympanic membrane to deliver the medicament across the membrane and into the middle ear. The medicaments delivered according to the methods of the invention include antibiotic, anti-viral, anti-fungal and anti-inflammatory agents that are useful in treatment and/or prophylaxis of middle ear infections and their sequelae.
CN103520168A Compound injection agent containing tiamulin hydrogen fumarate The invention relates to the technology that sucrose acetate isobutyrate is applied to preparation of an oily injection agent for animals, in particular to a technology which combines sucrose acetate isobutyrate with hydrogenated castor oil and is used for preparing a compound long-acting injection agent containing tiamulin hydrogen fumarate and ceftiofur hydrochloride. A dispersion medium of the compound injection agent is isopropyl myristate or benzyl benzoate or ethyl oleate or a mixture mixing more than one of isopropyl myristate, benzyl benzoate and ethyl oleate. The compound injection agent is good in sustained release effect, stable in character, good in histocompatibility and easy to prepare.
EP2774932A1 Novel compound contained in manuka honey and use of same The present description discloses a novel biologically active ingredient of manuka honey. Specially, the present description discloses a compound represented by the following formula. In this formula, each of R1, R2 and R3 independently represents a hydrogen atom or optionally substituted C1-4 alkyl group, m represents an integer from 1 to 3, each of R4-m, R5-m and R6-m independently represents a hydrogen atom or optionally substituted C1-4 alkyl group, and each of R7, R8, R9 and R10 independently represents a hydrogen atom or optionally substituted C1-4 alkyl group.
US20080249045 MGAL: A GAL Gene Switch-Based Suite of Methods for Protein Analyses and Protein Expression in Multicellular Organisms and Cells Therefrom The invention provides methods for detecting and analyzing protein-protein interactions and agonists and antagonists thereof, detecting and analyzing protein sequences, and regulatable gene expression in multicellular organisms or cells therefrom.
US20090004201 Therapy-Enhancing Glucan A therapeutic composition for treatment of cancer in a mammal is disclosed. The composition comprises an effective amount of a yeast beta-glucan composition which is suitable for oral administration and for absorption through the gastrointestinal tract of the mammal. The above therapeutic composition may further comprise antitumor antibodies or cancer vaccine composition, wherein the antitumor activities of the antitumor antibodies or the cancer vaccine composition are enhanced by the yeast glucan.
US20110091501 Recombinant Rhinovirus Vectors The invention provides rhinovirus vectors, which can be used in the delivery of immunogens, such as influenza virus immunogens, and corresponding compositions and methods.
WO2011095807A1 Combinations of mek and hh inhibitors The present invention relates to a therapeutic combination comprising a MEK inhibitor and an HH- pathway inhibitor, and to methods for the production of an anti- cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to: a therapeutic combination comprising a MEK inhibitor and an HH- pathway inhibitor; a combination product comprising a MEK inhibitor and an HH- pathway inhibitor, a kit of parts comprising a MEK inhibitor and an HH- pathway inhibitor; use of a therapeutic combination, combination product or kit of parts in the treatment of cancer; a method of treating cancer comprising administering the therapeutic combination, combination product or kit of parts to a patient. The therapeutic combination and methods of the invention are also useful in the treatment of conditions in which the inhibition of MEK and/or the HH-pathway is beneficial.
WO2013063216A1 5-nonyloxytrptamine and related intracellular ph acidifiers for the treatment and prevention of cancer Provided herein are compositions for lowering intracellular pH in a cell or population of cells from a subject comprising contacting the cell or population of cells with a therapeutically effective amount of 5-nonyloxytryptamine or a pharmaceutically acceptable salt, solvate, stereoisomer, or derivatives thereof. These compounds are useful for acidification of cells, including cancer cells, which induces apoptosis and cell necrosis. Methods of use of these compounds, including in in pharmaceutical compositions in conjunction with other biologically active agents, in treatment of cancers, including glioblastoma and related neuronal cancers are also included.
EP2318401A2 Azaindole inhibitors of iap The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: I wherein X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3', R4, R4', R5, R6, R6' and R9 are as described herein.
CN102883720A Method of treating pancreatic cancer A therapeutic method for treating pancreatic cancer is disclosed comprising administering to a patient in need of treatment a ruthenium complex salt.
EP1575924A1 4-substituted benzimidazoles and their use as inhibitors of gastric secretion The invention relates to 6-substituted benzimidazoles of formula 1, in which X is O (oxygen) or NH and Y has either the meaning -CH2-Ar wherein Ar is a mono- or bicyclic aromatic residue, or Y denotes the group gp, formula (gp) wherein Z has the meaning -CHR8- or -CHR8-CHR9-. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.
WO2006117624A3 Kynurenic acid and salts thereof for the prevention and treatment of shock The use in therapy of kynurenic acid and pharmaceutically acceptable salts there for preparing drugs effective in the prevention and treatment of shock, in particular septic shock, is described.
WO2013182274A1 Imidazo-oxadiazole and imidazo-thiadiazole derivatives The present invention provides compounds of Formula (I) used as Amyloid beta lowering agent for the treatment of neurodegenerative diseases.
CN101084943A Method for preparing mixture containing natural vitamin P from sea-buckthorn The invention relates to a method for preparing mixture containing vitamin P from sea buckthorn, and is for the prupose of providing a method for preparing a mixture containing 0.5-50% of vitamin P and 2-30% of vitamin C through extracting juice, degassing, enzyme-hydrolyzing, degreasing, homogenize, reducing acid, desugarizing, millipore filtering, freeze drying and pulverizing. The method is simple; solve the problem of brown stain of highly active substance in sea buckthorn due to high temperature oxidation by adopting biologic-physical method at low temperature, has no requirement of any solvent, no residue, low cost, and high biologically active substance yield. Vitamin P and vitamin C is in coexistence in the product, which promotes absorption.
WO2014046753A2 Method and system for treatment of biological tissue A composition for reconstruction, replacement or repair of damaged or diseased biological tissue comprising an extracellular matrix (ECM) composition that includes an ECM scaffold component and a bioactive agent component. In a preferred embodiment, the ECM scaffold component comprises mesothelial tissue and the bioactive agent comprises a statin.
CA2757190A1 Production method for ubiquinone powder for use in preparations and product thereof Disclosed are a production method for a ubiquinone powder for use in preparations, including Step 1 of compression molding a ubiquinone crystal powder at a linear molding pressure of from 0.6 to 2.5 tons/cm to obtain a compressed fragment; and Step 2 of grinding the compressed fragment obtained in Step 1 to obtain a powder; and a ubiquinone powder for use in preparations, which is obtained by the subject production method. According to the subject production method, it becomes possible to provide a ubiquinone powder for use in preparations for medicines and health foods, which has a high bulk density, a small angle of repose and excellent handling properties and fluidity, without using an additive such as an excipient, a binder and the like.
US20090047240 Chaperonin 10-induced immunomodulation The present invention relates to methods for modulating Toll-like receptor signalling in a subject, or in at least one cell, tissue or organ thereof, methods for treating or preventing a disease or condition in a subject, methods for modulating the production and/or secretion of one or more immunomodulators in a subject, or at least one cell, tissue or organ thereof, wherein said methods involve the administration of chaperonin 10, and wherein the chaperonin 10 associates with a Toll-like receptor in an activation cluster. Also contemplated are associated compositions and uses thereof.
DE102010026879A1 Transdermal system, useful for indicating and preventing multiple sclerosis, immunomodulator including quinolines or isoxazoles, metabolite forming groups, skin protective layer, a reservoir and a carrier impermeable to active substance Transdermal system comprises: at least one immunomodulator as an active substance including quinolines, isoxazoles, fumaric acid derivatives, sphingosine-1-phosphatase-receptor-modulators or their salts; metabolite forming groups; a skin protective layer impermeable to the active substance; an active substance reservoir; and a carrier impermeable to the active substance for the reservoir. - ACTIVITY : Neuroprotective; Anti-inflammatory; Gastrointestinal-Gen. - MECHANISM OF ACTION : Sphingosine-1-phosphatase-receptor-modulator.
US20110020438 Crystallization Inhibitor and Its Use in Gelatin Capsules The present invention describes soft gelatin capsules that encapsulate a water-insoluble active ingredient and an excipient composed of a crystallization inhibitor that stabilizes the water-insoluble inhibitor. The crystallization inhibitor being at least one mononacylglycerol compound whose acyl group is a fatty acid residue of 6-18 carbon atoms. The capsule contents are more resistant to turbidity, forming a coarse emulsion, and crystallization of the active ingredient compared with compositions absent the crystallization inhibitor.
WO2011090095A1 Heterocyclic compound having azole group A heterocyclic compound represented by general formula (I) [wherein R1 represents an optionally protected amino group, or an optionally substituted C1-6 alkyl group; R2 and R3 independently represent a C1-2 alkyl group; X represents a hydrogen atom, or a halogen atom; Z1 represents C-R4 (wherein R4 represents a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group), or N; Z2 represents C-R5 (wherein, R5 represents a hydrogen atom, a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group), or N; Z3 represents C-R6 (wherein R6 represents a hydrogen atom, a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group ), or N; Z4 represents C-R7 (wherein, R7 represents a hydrogen atom, a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group), or N; Z represents CH or N; and A represents a methylene group, or a bond] or a salt thereof, which has an excellent anti-HIV activity and is therefore useful as an anti-HIV agent.
WO2007135406A2 New forms of active pharmaceutical ingredient The present invention is concerned with new polymorphic forms of entacapone, in particular new polymorphic forms α, β, γ, δ, ε, τ and the amorphous form of entacapone, processes of preparing the forms, pharmaceutical compositions containing the same, therapeutic uses thereof and methods of treatment employing the same.
US20090176883 TRPA1 Antagonists Compounds of formula (I) wherein R1, R2, R3, m, and Y are defined in the specification are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
CN1861582A Cyclopropyl substituded triazol kind anti fungus compound and preparation process and use thereof A cyclopropyl substituted triazole alcohol kind of antifungus compounds used for preparing antifungus medicines and its preparing process are disclosed. Its advantages are high curative effect, low poison and broad spectrum.
US20100256218 RNAi MODULATION OF MLL-AF4 AND USES THEREOF The invention relates to compositions and methods for modulating the expression of the MLL-AF4 fusion gene, and more particularly to the downregulation of MLL-AF4 by chemically modified oligonucleotides.
US20120059036 Method for reducing thrombocytopenia and thrombocytopenia-associated mortality Disclosed are methods for reducing the risk of thrombocytopenia-associated mortality and morbidity, and for reducing the risk of becoming thrombocytopenic, in patients whose treatment requires inhibition of platelet aggregation. The methods involve administration of a pharmaceutically acceptable salt of tirofiban.
US20110135595 Neuregulin based methods and compositions for treating cardiovascular disease The present invention relates to compositions and methods for preventing, treating or delaying various cardiovascular diseases or disorders in mammals, particularly in humans. More particularly, the present invention provides for compositions and methods for preventing, treating or delaying various cardiovascular diseases or disorders using, inter alia, a neuregulin protein, or a functional fragment thereof, or a nucleic acid encoding a neuregulin protein, or a functional fragment thereof, or an agent that enhances production and/or function of said neuregulin.
WO2010121391A1 Solid food comprising dietary fiber and/or foodstuff rich in dietary fiber, preparation and use thereof A solid food comprising dietary fiber and/or foodstuff rich in dietary fiber，preparation and use thereof. The said solid food is made of materials comprising dietary fiber and/or foodstuff rich in dietary fiber, alginate, solidifying agent and water, and is made into multiple edible formulations.
CA2736441A1 Pyrazolylthiazole compounds as .delta.f508-cystic fibrosis transmembrane conductance regulator correctors The present disclosure provides compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The compositions pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The compositions and pharmaceutical preparations of the invention may comprise one or more pyrazolylthiazole-containing compounds of the embodiments, or an analog or derivative thereof.
WO2008011799A1 NEW USE OF NON-RECEPTOR TYROSINE KINASE c-Ab1 SPECIFIC INHIBITORS The new use of non-receptor tyrosine kinase c-Ab1 specific inhibitors alone or in combination with cisplatin or cyclophosphamide in preparing antitumor medicaments and / or auxiliary antitumor medicaments. Experiments prove that non-receptor tyrosine kinase c-Ab1 specific inhibitors can inhibit the activity of c-Ab1 kinase to lead the denaturation aggregation and lysosome degradation of Gal3 and to lower the Gal3 protein level in the tumor cells obviously, so as to kill tumor cells in autophagic apoptosis.
EP1628668A2 1,1-disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, beta-aminoacids, alpha-aminoacids and derivatives thereof as factor xa inhibito rs The present application describes 1,1-disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, β-aminoacids, α-aminoacids and derivatives therof of Formula(I) or pharmaceutically acceptable salt forms thereof, wherein M is a linear core. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
CN101268078A Pyrazolo[3,4-b]pyridine compound, and its use as a pde4 inhibitor The invention provides 4-{[1-(aminocarbonyl)-4-piperidinyl]amino}-N-[(3,4-dimethylphenyl)methyl]-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carb oxamide, which is the compound of formula (I), or a salt thereof. The invention also provides the use of said compound or a pharmaceutically acceptable salt thereof as an inhibitor of phosphodiesterase type IV (PDE4), for example in the treatment and/or prophylaxis of an inflammatory and/or allergic disease, cognitive impairment or depression in a mammal. In particular, the invention provides the use of the compound or pharmaceutically acceptable salt in the treatment and/or prophylaxis of atopic dermatitis in a mammal, for example by external topical administration to the mammal such as a human. Pharmaceutical compositions containing said compound or salt, in particular suitable for external topical administration, are also provided.
CN101015571B Chinese caterpillar fungus polysaccharide buccal tablets and its preparing process The invention belongs to health products with immunity improving, anti tumour, antiaging effects, especially relates to buccal tablets prepared from Cordyceps sinensis as raw material. The buccal tablets comprises (by weight part) Cordyceps sinensis polysaccharide 15-35, sorbitol 20-50, mannit 25-45, microcrystalline cellulose 5-10, and carboxymethyl cellulose 3-7. The preparation method comprises pulverizing Cordyceps sinensis or Cordyceps Militaris, sieving with a sieve of 100 meshes, extracting with hot water of 95-100deg.C, precipitating with ethanol, concentrating, freeze drying or drying under reduced pressure, mixing with other materials, granulating, drying at 60deg.C, and tabletting to obtain the final product. The invention has antitumour, immunity increasing, and antiaging effects; has the advantage of convenient administration, and can be used as everyday health products for administration.
US20110039872 Deuterium-enriched capecitabine The present application describes deuterium-enriched capecitabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20080153838 Compounds Having Tie2 (Tek) Activity The invention relates to a compound of the Formula I. or salt, prodrug or solvate thereof, wherein R1, R5, R6, D, A, B, L, n, m and p are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.
US20100061991 Identification of therapeutic agents for HIV infection A cell surface molecule designated DCIR (for dendritic cells ImmunoReceptor), a member of a recently described family of DC-expressing C-type lectin receptors, has been shown to participate to the capture of human immunodeficiency virus (HIV) and promote infection in trans and in cis of autologous CD4(+) T cells from human immature monocyte-derived DC. The contribution of DCIR to these processes was revealed using DCIR-specific siRNAs and a polyclonal antibody specific for the carbohydrate recognition domain of DCIR. Therapeutic agents for HIV infection are therefore provided herein. These therapeutic agents are useful for impairing the interaction between DCIR and HIV and as such may be useful for treatment or prevention of HIV infection. Also provided are assays for identifying additional therapeutics agents for treatment or prevention HIV infection.
CN102302450A Hydrophobic drug-albumin-glucan nano emulsion, as well as preparation method and application thereof The invention belongs to the technical field of medicines, and particularly relates to a hydrophobic drug-albumin-glucan nano emulsion, as well as a preparation method and application thereof. In the structure of emulsion droplets in the nano-emulsion, an oil phase containing hydrophobic drug is taken as an inner core, albumin is an oil-water interfacial film, and glucan is positioned outside oildroplets to maintain the stability of the oil droplets in a water phase. The preparation method comprises the following steps: preparing an albumin-glucan covalent complex by utilizing Maillard reaction; dissolving the albumin-glucan covalent complex in an aqueous solution to obtain one solution; dissolving or dispersing the hydrophobic drug in soybean oil to obtain one solution; mixing the two solutions, and preparing an oil-in-water nano emulsion by a high-pressure homogenization method; and heating the prepared oil-in-water nano-emulsion to form a stable albumin oil-water interfacial film so as to obtain a stable drug-carrying nano emulsion. In the nano-emulsion, the protein oil-water interfacial film is stable, the emulsion droplets are not easily congregated, so that the requirement of an injection preparation can be fulfilled, and the nano-emulsion can be applied as a hydrophobic drug injection preparation.
US20090163454 Methods of Step-Down Hormone Treatment The present invention relates to methods of step-down hormone treatment in which an estrogen and progestin combination regimen is administered for one or more cycles prior to administration of a lower dose hormone regimen containing a lower daily dosage amount of estrogen and/or progestin.
WO2013153539A1 Tricyclic compounds as tec kinase inhibitors The present invention is directed to tricyclic compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by ITK.
CN102078331A ICCB-containing compound preparation and preparation method thereof The invention provides an ICCB-containing (in-vitro-cultured calculus boris) compound preparation which comprises the following components in parts by weight: 0.5 to 2 parts of ICCB, 20 to 30 parts of acetaminophen, 8 to 15 parts of amantadine hydrochloride, 0.1 to 0.4 parts of chlorpheniramine maleate, 1.0 to 2.5 parts of caffeine, and the appropriate amount of sucrose and food flavors auxiliary materials. By using the ICCB compound preparation instead of artificial bezoar, the side reactions in which vomit and jaundice symptoms are caused by over high free bilirubin contained in artificial boris can be reduced; medicament ingredients can be effectively dispersed with an equivalent increment method to mix and grind, thereby reducing side effects caused due to uneven contents of chlorpheniramine maleate, chlorpheniramine maleate and amantadine hydrochloride.
EP1813272A1 Veterinary use of a lleuromutilin derivate againts ileitis in swine Use of the compound of formula in the therapy of a veterinary disease the expression of which is enhanced by increasing stocking density, and wherein the veterinary disease is ileitis in swine associated with Lawsonia intracellularis infection
US20080286224 Use of a Lotion Composition on an Absorbent Article for Reducing Adherence of Feces or Menses to the Skin The present invention relates to lotion compositions comprised on a body facing surface of an absorbent article such as a diaper, training pants or adult incontinence product. The lotion composition reduces the adherence of feces or menses to the human skin. The lotion composition comprises at least two compounds wherein one first compound is liquid at 25° C. and at least one second component which is solid at 25° C. An effective amount of the lotion composition is comprised on a body facing surface of an absorbent article which is intended to be worn by a wearer.
US20080044457 Antitumor agents; time-release agents; pulverization The present invention discloses general formula I of Temozolomide-8-carboxylate compounds, the process for preparation, pharmaceutical compositions comprising the compounds and the use of the compounds and pharmaceutical compositions for the manufacture of an antitumor medicament. The said pharmaceutical composition comprises one or more general formula I Temozolomide-8-carboxylate compounds as active ingredient, together with conventional pharmaceutical carriers. The composition also comprises one or more pharmaceutically acceptable acidic material, optionally second or tertiary alcohol or ester or ether derivatives thereof. The said pharmaceutical composition can be made into various common formulations, particularly oral formulations as well as topically transdermal patches. The present invention also discloses the application of the compounds and the compositions to treat tumor.
WO2014076091A1 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
WO2006044556A3 Dual inhibitors of lipoxygenase for treating diabetes Disclosed are methods for the treatment of diabetes by administering a composition comprising a pharmaceutically acceptable amount of a dual inhibitor of both 5 -lipoxygenase (5-LO) and 12/15 -lipoxygenase (12/15-LO) enzymes or of both 5 -lipoxygenase (5-LO) and 15 -lipoxygenase (15-LQ) enzymes. The invention is also directed to methods of controlling blood glucose level in diabetic patients with a dual inhibitor of both 5 -lipoxygenase (5-LO) and 12/15 -lipoxygenase (12/15-LO) enzymes or of both 5 -lipoxygenase (5-LO) and 15 -lipoxygenase (15-LO) enzymes, such as nordihydroguaiareitic acid (NDGA) .
CA2528438A1 P-38 inhibitors Provided are aminoaryl substituted 5-membered heterocycle-based p38 kinase, including p38alfa and p38beta. Pharmaceutical compositions containing the compounds are also provided. Method of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
CN103536560A Ceftezole sodium composition powder for injection The invention provides a ceftezole sodium composition powder for injection, and belongs to the field of medicine and medicine preparation technology. The ceftezole sodium composition powder comprises following raw material ingredients, by weight, 7.26 to 9.17 parts of ceftezole sodium, 5.78 to 7.67 parts of chitosan nanoparticle, and 81.38 to 87.10 parts of injection water. Advantages of the ceftezole sodium composition powder are that: 1) in vitro antibacterial activity spectrum is wider, and poor antibacterial activity of ceftezole sodium on pneumococcus, pseudomonas aeruginosa and acinetobacter is improved greatly; 2) the nanoparticle medicine carrier is capable of changing membrane transport mechanisms, and increasing medicine permeability against biological membranes, and is beneficial for exhibition of pharmacological functions in cells; 3) ceftezole sodium coated by the nanoparticle carrier is rapidly gathered at primary organs, such as liver and spleen, of the reticuloendothelial system along veins, so that toxicity caused by nonspecific gathering of medicine is reduced; and 4) the chitosan nanoparticle can be used as a freeze-dried skeleton agent of the freeze-dried powder injection instead of mannitol so as to avoid active effects of mannitol on human bodies.
CN101273046B Indol-3-yl-carbonyl-azaspiro derivatives as vasopressin receptor antagonists This invention relates to indol-3-yl-carbonyl-azaspiro derivatives which act as Via receptor antagonists and which are represented by Formula (I) wherein the azaspiro-head group A and the residues R<1>, R<2> and R<3> are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in medicaments against dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.
WO2002042319A9 2-substituted estrogens as antiangiogenic agents Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula (I), wherein the variables are defined in the specification.
WO2011124713A1 Labelled huprine derivatives and their use in medical imaging The present invention concerns new Huprine derivatives of formula I: wherein R comprises a fluorophore or a nuclear probe and their use in medical imaging and in radiotherapy.
EP0952772B1 Methods of use of mononuclear phagocytes to promote axonal regeneration Methods and compositions for the use of allogeneic mononuclear phagocytes to promote axonal regeneration in the central nervous system of a mammal are disclosed. In one embodiment, allogeneic mononuclear phagocytes are cultured together with stimulatory tissue, such as dermis or at least one nerve segment, and are subsequently administered into the central nervous system of a mammal at or near a site of injury or disease. In an alternative embodiment, autologous monocytes, preferably stimulated autologous monocytes, are administered into the central nervous system of a mammal at or near a site of injury or disease. Methods for identifying stimulatory tissue and cells and methods and compositions for cryopreserved allogeneic mononuclear phagocytes are also disclosed.
CN101889982A Novel long-circulating liposome composition and preparation method thereof The invention relates to a novel long-circulating liposome composition and an application method thereof. The long-circulating liposome composition is mainly prepared from phospholipid, cholesterol, an electronegative material and a long-circulating material serving as main raw materials, wherein tocopheryl acetate succinate or cholesterol succinate is used as the electronegative material particularly, and tocopheryl acetate polyethylene glycol succinate (TPGS) is used as the long-circulating material particularly, so that the stability of combining the long-circulating liposome composition and medicaments is improved; the long-circulating liposome composition can be used as a carrier of anti-tumor medicaments such as paclitaxel, docetaxel and 10-hydroxycamptothecine, and simultaneously, the tolerance is improved; and when the long-circulating liposome composition is used as the medicinal carrier, the circulating time of the carried medicaments in vivo is longer than that of various carriers sold on the market obviously, and the long-circulating liposome composition has the advantages of low cost and suitability for wide popularization and application.
CN102040603A Brominated N-o-methoxycarbonylbenzyl tetrahydroberberine and application thereof in treatment of hyperlipidemia The invention discloses brominated N-o-methoxycarbonylbenzyl tetrahydroberberine and application thereof in treatment of hyperlipidemia. The structure of the brominated N-o-methoxycarbonylbenzyl tetrahydroberberine is shown as the formula (I). The invention also discloses a synthesis and preparation method for the compound, a medicament composition containing the compound, application of the compound in treatment of hyperlipidemia, or application of the compound in treatment of hyperlipidemia by combining other blood fat regulating medicaments.
WO2005108337A2 Compounds with activity at estrogen receptor Disclosed herein are novel di-phenyl compounds and methods for using various di-phenyl compounds for treatment and prevention of diseases and disorders related to estrogen receptors.
WO2009128955A1 Treatment of inflammatory bowel disease with 6-mercaptopurine Methods of administering a delayed release 6-mercaptopurine pharmaceutical composition to patients suffering from inflammatory bowel disease which provide for release of the 6-mercaptopurine after passage of the pharmaceutical composition through the stomach are disclosed. The methods result in significant clinical improvement despite leading to very little systemic absorption of 6-mercaptopurine and also result in very few undesirable side effects.
WO2005118811A1 Novel polypeptide useful for diagnosis and treatment of cancer A novel cancer marker is found, and there is provided a method of effectively detecting cancer. Further, there is provided a pharmaceutical composition for cancer prevention or treatment. In particular, there is provided a method of detecting cancer through detection of U7 polypeptide expression effected in a sample taken from a test subject.
US20100298206 Hybrid oligomers, their preparation process and pharmaceutical compositions containing them The present invention relates to compositions and methods for producing therapeutic oligomeric compounds. In one aspect the invention relates to methods for administering the oligomeric compounds for the treatment and prevention of disease, for example, a fungal infection, bacterial infection, or cancer, in a mammal. In particular, the invention relates to medicaments comprising various novel oligomeric compounds and pharmaceutically acceptable salts thereof. The compounds of the invention may optionally be administered with at least one of a pharmaceutically acceptable excipient, pharmacologically active agent or a combination thereof.
CN101112360A Allicin fatty milk injection and preparation technics thereof The invention discloses an allicin fat emulsion injection and a preparation process thereof; the invention is the drug which is made by the materials with the following mix ratios by weight, while the pH value of which is 6.5 to 7.5, the average particle size of the emulsion particles is 200nm, and the particle size thereof is 100 to 300nm and the Zeta potential is minus 50 to 80mv. The raw materials are: allicin, egg yolk lecithin, pluronic F68, oleic acid, and injection water and so on. The preparation process is that the egg yolk lecithin, oleic acid, vitamin E and soya bean oil are taken at first under the aseptic conditions for mixing, heating, agitating and dissolving, then the allicin is added to agitate till dissolution, and the filtrate can be obtained after the pressure filtration by a microporous membrane; the glycerol is taken at first and the injection water, disodium ethylene diamine tetraacetate and pluronic F68 are added for mixing and agitating till the dissolution, then the filtrate can be obtained after the pressure filtration by the microporous membrane; after the mixture of the two filtrates, a high speed agitator is used for agitating, the product is finally obtained through a high pressure homogenizer. The invention is characterized by no irritating effect and good stability, etc.
EP2450047A1 Pharmaceutical composition containing ephedrae for treating bronchitis and preparation method therefor A pharmaceutical composition for treating bronchitis and preparation method thereof. Said pharmaceutical composition consists of EPHEDRAE HERBA, GYPSUM FIBROSUM, FORSYTHIAE FRUCTUS, SCUTELLARIAE RADIX, MORI CORTEX, ARMENIACAE SEMEN AMARUM, PEUCEDANI RADIX, PINELLIAE RHIZOMA, etc. Said pharmaceutical composition is useful in relieving cough, eliminating phlegm, relieving asthma and resisting inflammation, so it has good curative effects on the acute tracheobronchitis.
US20120149752 Kit for balancing neurotransmitter levels The teachings provided herein generally relate to formulations, systems, and methods that have the ability to remit deficiencies and imbalances in a subject's serotonin and dopamine levels. The teachings relate to the preparation and uses of a formulation comprising a serotonergic agent or dopaminergic agent in a form capable of oral transmucosal delivery to a subject. The formulation includes a flavoring agent and a carrier base. The flavoring agent functions as a taste indicator of the endpoint of a taste titration of the serotonergic or dopaminergic agent for a subject receiving an oral administration of the formulation in the form of a taste titration, and the endpoint is indicated to the subject by a change in the intensity of the flavor of the flavoring agent.
US7378408 Methods of treatment and formulations of cephalosporin Formulations containing an antibacterial alkali metal salt of a cephalosporin compound and methods of treating bacterial infections in dogs and cats.
WO2007108071A1 Antistress composition and food and drink containing the same An antistress composition of the invention contains Ϝ-aminobutyric acid and a nucleic acid-related compound as active ingredients and it preferably contains Ϝ-aminobutyric acid and the nucleic acid-related compound in a mass ratio of 1:0.0001 to 1:0.1. The nucleic acid-related compound is preferably at least one type selected from the group consisting of uracil, uridine, uridylic acid (UMP), uridine 5’-diphosphate (UDP), uridine 5’-triphosphate (UTP), adenine, adenosine, adenylic acid (AMP), adenosine 5’-diphosphate (ADP), adenosine 5’-triphosphate (ATP), inosine, inosinic acid (IMP), inosine 5’-diphosphate (IDP), inosine 5’-triphosphate (ITP), deoxyuridine, deoxyuridylic acid (dUMP), deoxyuridine 5’-diphosphate (dUDP), deoxyuridine 5’-triphosphate (dUTP), deoxyadenosine, deoxyadenylic acid (dAMP), deoxyadenosine 5’-diphosphate (dADP), deoxyadenosine 5’-triphosphate (dATP), deoxyinosine, deoxyinosinic acid (dIMP), deoxyinosine 5’-diphosphate (dIDP), deoxyinosine 5’-triphosphate (dITP), xanthin and salts thereof. The antistress composition of the invention efficiently suppresses/decreases mental fatigue by oral intake, can be expected to have an effect of preventing/improving health disorder caused by the mental fatigue and can be easily formulated into various foods and drinks.
CN1634083A Orally disintegrating tablet of aspirin The invention relates to aspirin oral disintegrating tablet and its preparation process, wherein the orally disintegrating tablet comprises physiological effective dose of enteric-coated aspirin and pharmaceutically acceptable carrying agents suitable for preparing orally disintegrating tablet, which comprises macromolecular material, bulking agent, crumbling agent, effervescent agent, lubricating agent, flavoring agent, and other pharmaceutically acceptable carrying agents suitable for preparing orally disintegrating tablet.
US20070275952 Tie-2 Modulators and Methods of Use The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Tie-2. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.
WO2008005303A3 Thiazolopyrimidine modulators of trpv1 Certain TRPV1-modulating thiazolopyrimidine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
CN102731565A Water-soluble derivative of diphenylethene compounds, preparation method and usage thereof The invention belongs to the field of antineoplastic compounds and relates to a water-soluble derivative of diphenylethene compounds, especially a water-soluble derivative of trans-4-[2-(3,5-dimethoxyphenyl)vinyl]-1,2-benzenediol as shown in the formula I, a preparation method and a usage thereof in the preparation of antitumor drugs. The water-soluble derivative of diphenylethene compounds is prepared through water-soluble reconstruction by taking the compound, trans-4-[2-(3,5- dimethoxyphenyl)vinyl]-1,2-benzenediol, as a parent nucleus. Results of in vitro antineoplastic tests show that the water-soluble derivative of diphenylethene compounds has significant effects in inhibiting brain glioma cells SF188 and U87wt, breast cancer cells MCF-7wt and large cell lung cancer cells H460. The activity of the cells decreases along with the increase of drug concentration. The derivative disclosed by the invention is an effective antitumor agent and further, the derivative can be used for preparing the antitumor drugs.
US20100144589 Methods of predicting cancer lethality using replikin counts The present invention provides methods of predicting the relative growth rate, replication rate, or lethality of a first malignancy as compared to another malignancy or as compared to a plurality of malignancies, including methods of predicting the relative growth rate, replication rate, or relative lethality of a primary malignancy as compared to a metastatic malignancy, including comparing the concentration of Replikin sequences in the first malignancy with the concentration of Replikin sequences in another malignancy or malignancies and further provides Replikin peptides and Replikin Peak Genes identified within a malignancy for diagnostic, therapeutic, preventive, and predictive purposes.
CN102796052A Paeonol-1,2,3-triazole compound having antifungal activity and preparation method thereof The invention discloses a paeonol-1,2,3-triazole compound having antifungal activity and a preparation method thereof. Key points of the technical scheme of the invention are that: the two structural formulae of the paeonol-1,2,3-triazole compound having antifungal activity are shown in the specifications respectively. The invention further discloses a preparation method and an application of the compound. A paeonol-1,2,3-triazole compound of two types of structures is synthesized, has excellent antifungal performance, and can be well applied to prevention and control of animal and plant diseases caused by fungi; and moreover, a process in a preparation process is simple and is easy to control, and the product yield of a target product is high.
EP1344777B1 Imidazole derivatives, process for their preparation and their use Provided are compounds which have steroid C17,20 lyase inhibiting effect and are useful as preventive or therapeutic agents for prostatism and tumors including breast cancer. Specifically, compounds represented by the general formula (Ia) or (Ib), or salts thereof: (Ia) (Ib) wherein R is hydrogen or a protecting group; R1 is lower alkyl or cycloalkyl; and A and B are each an optionally substituted 5- or 6-membered ring bearing an amide linkage in the ring.
WO2010037252A1 Sulfated derivative of gastrodia elata polysaccharide, preparation method and use thereof A sulfated derivative of gastrodia elata polysaccharide which is extracted from gastrodia elata, preparation method and use in manufacturing an antitumor agent thereof are provided, wherein the structure of the gastrodia elata polysaccharide is as follows, wherein x and y are integer and x+y=16, n is integer; and it has a peak molecular weight of 2.8×105 and a specific rotation of +95˚ in 0.5 mg/ml aqueous solution; and the sulfated derivative of gastrodia elata polysaccharide is mainly the sulfated derivative of G.elatapolysaccharide on 6-hydroxy, and it has a peak molecular weight of 6.5×104 and a specific rotation of +150.0˚ in 0.5 mg/ml aqueous solution. The data of in vitro test shows that the sulfated derivative of said polysaccharide can inhibit angiogenesis by inhibiting Id1 expression, and thus inhibit tumor growth. Therefore, the sulfated derivative of said polysaccharide has a evident antitumor effect, and it has very little toxic effect on endothelial cell, so it can be used as an antitumor medicine.
CN1931163A Nanometer clotrimazole emulsion medicine and its prepn process The nanometer clotrimazole emulsion medicine consists of surfactant, oil, clotrimazole and distilled water. Its preparation process includes the following steps: weighing surfactant with or without co-surfactant; calculating HLB value and selecting oil for reaching emulsifying HLB value near that of the surfactant phase; dissolving clotrimazole into surfactant; changing the ratio between the surfactant phase and the oil phase regularly; adding distilled water slowly at 20-25 deg.c to form clear and flowing O/W type stable nanometer emulsion liquid. The nanometer clotrimazole emulsion has high skin permeability, no contamination to clothing, high dissolubility of clotrimazole, raised bioavailability of clotrimazole, delayed metabolism time and wide medicine market foreground.
CA2228221C Papillomavirus polyprotein constructs A papillomarivus polyprotein construct comprises at least two amino acid sequences fused directly or indirectly together, each of the sequences being the sequence of an early ORF protein of papillomavirus or an immunogenic variant or fragment thereof, and at least one of said sequences being other than the E6 or E7 protein sequence or an immunogenic variant or fragment thereof. Nucleic acid molecules encoding the polyprotein construct, prophylactic or therapeutic compositions comprising the polyprotein construct or the nucleic acid molecule, and methods for eliciting an immune response against papillomarivus in a host animal are also provided.
CN101234109A Pharmaceutical composition containing (3R, 2í»S)-3-(2í»-hydroxy-2í»-cyclopentyl-2í»-phenylethoxy) quinuclidine hydrochloride and uses thereof The invention discloses medical composition containing active component of (3R, 2'S)-3-(2'-hydroxyl-2'-cyclopentyl-2'-phenylethoxy) quinine quinuclidine chloride and application of the medical composition in preparing drugs for treating chronic obstructive lung disease, incontinentia urinae, diversified shock diseases and preparing adjuvant drugs used before anaesthesia. The active component of the medical composition of the invention has high optical purity, strong stereoselectivity in vivo process, definite curative effects and high pertinency to the disease, thus effectively avoiding generation of toxic and side effects.
CN101530401A Compound transdermal patch used for curing acute and chronic inflammatory pain The invention discloses a compound transdermal patch used for curing acute and chronic inflammatory pain. The patch comprises a compound penetrating agent and a pressure sensitive adhesive and is characterized by also comprising Xylocaine or hydrochloride thereof and sodium salt or sylvite of diclofenac. The transdermal patch contains the following components by weight percentages: 1-20 percent of Xylocaine or the hydrochloride thereof, 1-20 percent of the sodium salt or sylvite of diclofenac, 1-30 percent of compound penetrating agent and 40-49 percent of pressure sensitive adhesive. Aiming at overcoming the defects of the existing medicinal preparations in treatment and use, the invention provides a compound transdermal patch that is used for curing acute and chronic inflammatory pain, can act on local human body and quickly permeate, and is good in treatment effect, safe and convenient in use.
CN101590243A Application of small RNAs in preparing medicaments for treating and/or preventing lymphoma The invention relates to application of small RNAs in the field of preparing medicaments for treating and/or preventing lymphoma, in particular to the application of small RNA-15a, small RNA-16-1, precursor of the small RNA-15a and precursor of the small RNA-16-1 or a mixture of more than two of the small RNA-15a, the small RNA-16-1, the precursor of the small RNA-15a and the precursor of the small RNA-16-1 in preparing the medicaments. The over expression of the oligonucleotide array sequences in lymphomatous cells proves that the oligonucleotide array sequences have effects of inhibiting the growth of the lymphomatous cells and promoting the apoptosis of the lymphomatous cells and further discloses that the use of the oligonucleotide array sequences in combination with chemotherapeutics such as cytarabine can strengthen the efficacy of original medicaments, thereby ensuring the application potential of the oligonucleotide array sequences in the field of preparing the medicaments for treating and/or preventing lymphoma. The medicaments can be a single composite containing an oligonucleotide array sequence or mixture of the oligonucleotide array sequences and a pharmaceutically carrier or a chemotherapeutic-containing composite for use in combination.
WO2013053015A1 Meloxicam based formulations for providing analgesia in sheep The present invention provides a method of using meloxicam to provide analgesia or control inflammation in sheep wherein the method comprises administering the sheep a therapeutically effective amount of a formulation containing pharmacologically acceptable meloxicam or meloxicam salt. More preferably the method involves administering it to sheep undergoing a painful surgical procedure including one or more of: (i) tail docking, (ii) castration, (iii) muiesing. The formulations provided are adapted for administration via the oral and buccal route and preferably administered to the sheep is in the range of 0.25mg/kg to 1.Omg/kg of bodyweight of the sheep. The formulations provided have a concentration of meloxicam or meloxicam salt between 0.25% and 1 % (w/v) which when administered, result in a C max plasma concentration of meloxicam in the sheep of at least 750 mg/ml. The formulations provided include liquid gels, liquid suspensions and liquid solutions.
EP1736470A2 Pyrimidine derivatives as CB2 cannabinoid receptor modulators The present invention relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
US20100166893 Herbal composition for reducing add/adhd and method thereof Disclosed herein is a herbal composition comprising supercritical fluid extracts/oils of Jyotishmati, Bacopa monnieri, Ginger Oil, Flax Seed oil, Rosemary Ext and Vitamin E in an effective amounts useful in the treatment of symptoms associated with Attention Deficit disorder (ADD) and Attention deficit/hyperactivity disorder (ADHD).
US20080076794 Hyperaldosteronism The application relates to novel heterocyclic compounds of the general formula (I) in which R, R1, R2, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
EP1854466A1 Pharmaceutical composition comprising a combination of calcitriol and clobetasol propionate The present invention relates to pharmaceutical compositions in the form of a gel, a cream, a lotion, a solution or an ointment comprising, in a pharmaceutically acceptable medium, at least calcitriol and clobetasol propionate, and to the use of those compositions for the preparation of a medicinal product for treating dermatological complaints such as psoriasis, atopic dermatitis, contact dermatitis and seborrhoeic dermatitis.
EP1725244B1 Method of preventing fibrin clots in pulmonary tissue through the use of aerosolized anticoagulants ATIII is a serine proteinase inhibitor (serpin) with anti-coagulant, anti-inflammatory, anti-proliferative and anti-angiogenic properties. The invention features methods of treating a subject having lung injury due to bums and smoke inhalation by administering a synergistic combination of antithrombin III and heparin through pulmonary delivery means.
CN101264093A Compositions for increasing energy in vivo The invention relates to a composition comprising ribose for increasing energy in vivo in purpose of preparing medicine composition orally to mammals with 0.1-20g ribose daily dosage for increasing mammals energy level. Precursors of adenosine triphosphate are administered orally to increase intracellular ATP concentration as dietary supplements or for treatment of reduced energy availability resulting from strenuous physical activity, illness or trauma. Pentose sugars are administered individually, mixed into dry food or in solution. The preferred pentose is D-ribose, singly or combined with creatine, pyruvate, L-carnitine and/or vasodilating agents. Additionally, magnesium, electrolytes, fatty acids and hexose sugars can be used. The compositions and methods of this invention are especially beneficial to mammals having reduced energy availability or high energy demand.
WO2013177224A1 N-substituted benzamides and their use in the treatment of pain The invention provides novel compounds having the general formula (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
CN103304537A Biphenyl cyclooctene lignans compound as well as preparation method and application thereof The invention discloses a biphenyl cyclooctene lignans compound as well as a preparation method and application thereof. The biphenyl cyclooctene lignans compound is obtained by separating from branches, leaves and fruit of dry Yunnan-Tibet schisandra chinensis, and has the structure shown in the specification; the preparation method of the biphenyl cyclooctene lignans compound is as follows: performing extracting, silicagel column chromatography and high performance liquid chromatography separation on the branches, leaves and fruit of dry Yunnan-Tibet schisandra chinensis used as raw material; the method comprises the following specific steps of: crushing and extracting the branches, leaves and fruit of dry Yunnan-Tibet schisandra chinensis, filtering, reducing pressure and concentrating as an extract, extracting, performing the silicagel column chromatography on an extract phase, performing gradient eluting by using the organic solution in a volume proportion of (1:0)-(0:1), further performing the inverse-phase column chromatography and high performance liquid chromatography separation and purification on 9:1 part of the eluant to obtain the biphenyl cyclooctene lignans compound. According to the evidence, the biphenyl cyclooctene lignans compound disclosed by the invention is provided with good HIV-1 activity, the compound is novel in structure, good in activity and can be used as the pilot compound of anti-AIDS drugs.
CN102614156A Medical application of in-vivo metabolite of paeonol The invention belongs to the field of medical application and particularly relates to an in-vivo metabolite of paeonol and the medical application of the in-vivo metabolite of paeonol. A metabolite is obtained by separating collected urine of a testee who orally takes paeonol tablets by means of macroporous adsorption resin column chromatography, medium and low pressure octadecyl silane (ODS) column chromatography, SephadexLH-20 column chromatography, preparative high performance liquid chromatography (PHPLC) and the like through high performance liquid chromatography (HPLC)/personal digital assistant (PDA) track detection. The chemical structure of the metabolite is 2,5-dyhydroxyl-4-methoxyacetophenone which is identified by means of electrospray ionization mass spectrometry (ESI-MS), 1 hydrogen-nuclear magnetic resonance (1H-NMR), 13 carbon-nuclear magnetic resonance (13C-NMR), nuclear overhauser effect spectroscopy (NOESY) and the like. Experiments show that the metabolite is higher than the paeonol in biological activity in inhibiting lipopolysaccharide-induced mouse mononuclear macrophage from synthesizing nitric oxide (NO) in vivo and clearing hydroxyl free radical (OH), so the metabolite can be used for preventing and/or treating human and animal inflammation and diseases related to excessive hydroxyl free radical (OH).
WO2011091614A1 7-(2-substituted-3-amino-1-tetrahydropyrrolo[3,4-c]pyrazolyl)quinoline carboxylic acid derivatives, their preparation methods and uses against bacterium and tuberculosis 7-(2-substituted-3-amino-1-tetrahydropyrrolo[3,4-c]pyrazolyl)quinoline carboxylic acid derivatives, their preparation methods and uses against bacterium and tuberculosis are disclosed. 7-(2-substituted-3-amino-1-tetrahydropyrrolo [3,4-c]pyrazolyl)quinoline carboxylic acid derivatives are compounds shown by formula I, pharmaceutically useful salts, physiologically hydrolysable esters, hydrates or isomers thereof. They have unexpected high antibacterial and antitubercular activities, and compared with antibacterial and antitubercular quinolones medicines which are available on the market, they have superior wide-spectrum antibacterial activities and antitubercular activities. Thus, they have a prospective future in preparing antibacterial medicines or antitubercular medicines.
US7560472 1-cyclohexylethyl ammonium salts; for inhibiting gastric juice secretion The present invention relates to new salts of the single enantiomers of omeprazole, i.e. salts of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole ((S)-omeprazole) and (R)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole ((R)-omeprazole) respectively. More specifically, the present invention relates to 1-cyclohexylethyl ammonium salts of the compounds, formed by a reaction of (S)-omeprazole and (R)-omeprazole respectively and 1-cyclohexylethyl amine. The present invention also relates to a process for preparing the compounds of the invention, a pharmaceutical preparation and a method for treatment of gastric related disorders by administering the compounds of the invention.
US20060127481 Ophthalmic drug delivery system using polymer micell The current situation is such that it is difficult for drugs to reach posterior tissues of eyeball, such as choroid and retina, with the result that treating diseases in such regions is difficult. Thus, how to attain effective delivery of drugs is of importance. It has been found that effective delivery of drugs to positerior tissues of eyeball, such as choroid and retina, especially those wherein vascularization has occurred can be accomplished by systemic administration, especially intravenous administration of polymer micells having a drug incorporated therein. Further, it has been found that when a photosensitive substance is used as a drug and PDT is carried out, choroidal neo-vessels can be effectively choked so as to be useful for the treatment of age-related macular degeneration.
WO2009047928A1 Method of producing functional dna, transformant and remedy for disease It is intended to provide a method of producing a functional DNA whereby the functionality of DNA can be further improved, a transformant which has this DNA transferred thereinto, and a remedy for a disease which contains the functional DNA. A method of producing a functional DNA which comprises the procedure of applying an ultrahigh hydrostatic pressure to a starting DNA in a liquid to thereby construct a condensed DNA. Owing to this procedure, the transfer efficiency of the DNA into a cell can be elevated and the expression efficiency thereof in a cell can be elevated simultaneously.
WO2006078907A1 2-substituted benzimidazole derivatives as vanilloid receptor ligands and their use in treatments Substituted benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
WO2010097201A1 Serine palmitoyltransferase inhibitors for preventing and delaying retinitis pigmentosa The present invention relates to the use of serine palmitoyltransferase inhibitors for preventing and delaying inherited retinal degenerations, and compositions which contain them.
US7034026 serine/threonine kinase inhibitors; 2,3-diphenylquinoxalines in which at least one of the phenyls is substituted with an amine group, particularly 2-[4-(2-aminoprop-2-yl)phenyl]-3-phenylquinoxaline; treating cancer The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention
EP1666062A2 Therapeutic applications for the anti-T-BAM (CD40-L) monoclonal antibody 5c8 Activation of cells bearing CD40 on their cell surface by CD40 ligand is inhibited by contacting the cells with an agent capable of inhibiting interaction between CD40 ligand and the cells, in an amount effective to inhibit activation of the cells. Activation of cells bearing CD40 on their surface by CD40 ligand in a subject is inhibited by administering to the subject an agent capable of inhibiting interaction between CD40 ligand and the cells, in an amount effective to inhibit activation of the cells. Conditions dependent on CD40 ligand-induced activation of CD40-bearing cells are treated.
WO2006042103A3 Reversible inhibitors of cathepsin b The present invention is directed to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6a are as that are inhibitors of cathepsin B and are as in the description, that are inhibitors of cathepsin B and are therefore useful in treating diseases, disorders, or syndromes mediated by this cathepsin. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
CN101919853A Pharmaceutical composition, preparation method and application thereof The invention relates to a pharmaceutical composition, a preparation method and application thereof. The invention provides a sustained release capsule which contains fexofenadine or pharmaceutically acceptable salt thereof and pseudo-ephedrine or pharmaceutically acceptable salt thereof, wherein the pseudo-ephedrine or the pharmaceutically acceptable salt thereof is a sustained release part, and the fexofenadine or the pharmaceutically acceptable salt thereof is an ordinary release part. The invention also provides the preparation method of the sustained release capsule and the application of the capsule in preparing drugs for treating allergic rhinitis, chronic urticaria and influenza. Compared with tablets, the sustained release capsule is easy to be absorbed, and has the advantages of rapid action, smaller individual difference of blood concentration, less irritation on gastrointestinal tracts, less possibility of drug collapse, good safety and larger dose flexibility.
CN101805309A Benzamide derivatives useful as histone deacetylase inhibitors The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R<1> is a group such as hydroxy, halo, trifluoromethyl and cyano; R<2> is halo and n is 0-2; and each R<4> is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R<3> is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.
WO2011116356A3 Positive allosteric modulators of group ii mglurs The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive ailosteric modulators of the melabotropic glutamatc subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.
CN102727435A Aqueous chlorhexidine iodine sterilizing spray and preparation method thereof The invention relates to aqueous chlorhexidine iodine sterilizing spray and a preparation method thereof. The spray comprises the following materials by weight: 0.1-2% of chlorhexidine iodine, 1-30% of solubilizer, 0.5-5% of cosolvent and the balance of water, and is prepared by dissolving the chlorhexidine iodine, the solubilizer and the coslovent with appropriate amount of water under ultrasonic treatment, adding the rest of water until the sum of the prescription is 100%, mixing, and filling into a spray bottle. The inventive spray has the advantages of no iodine odor, yellow-staining, toxicity, teratogenecity and skin/mucous membrane irritation, low available concentration, strong sterilizing ability, wide antibacterial spectrum, simple preparation process, and easy popularization.
EP1313736B1 Condensed pyrazindione derivatives as inhibitors of pde5 Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents. In particular, the invention relates to compounds that are potent and selective inhibitors of cyclic guanosine 3', 5'-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5.
US20090022818 High-foaming, viscous cleanser composition with a skin care agent A liquid cleansing composition comprising a cleansing surfactant, an adsorbed skin-care agent, adsorptive polymeric particles having an adsorption capacity of at least 2 g of skin care agent per gm of dry polymeric particles, a polymeric thickening agent having a molecular weight in the range of 500,000-10,000,000 Dalton, a water-soluble polymer having a molecular weight in the range of 200-50,000 Dalton, and a hydrophilic liquid, the said cleansing composition having the following features i) the low molecular weight, water-soluble polymer component functions as a foam-boosting and thixotropy-boosting agent; ii) the ratio of the Brookfield viscosity at 1 rpm of spindle speed to the Brookfield viscosity at 100 rpm of spindle speed is at least 10; and iii) the foam-volume is at least 20% higher with the water-soluble, polymeric, foam-boosting component than without it.
CN101273969A Compound anticancer sustained-release agent containing Clofarabine A compound anti-cancer sustained-release injection containing clofarabine is composed of sustained-release microspheres and a solvent, wherein, the sustained-release microspheres comprise anti-cancer effective components and sustained-release excipients, the anti-cancer effective components are composed of the clofarabine and a clofarabine synergist which is selected from anti-tumor antibiotics and/or anti-metabolism drugs, the solvent is the special solvent containing a suspending agent; the sustained-release excipients are selected from polylactic acid/glycolic acid copolymer, monomethyl polyethylene glycol/polylactic acid, polyethylene glycol/polylactic acid, terminal carboxyl polylactic acid, terminal carboxyl polylactic acid/glycolic acid copolymer, EVAc, copolymer of fatty acid and sebacic acid and so on; the viscosity of the suspending agent is 80cp to 3000cp ( at 20 DEG C to 30 DEG C ), and the suspending agent is selected from carboxymethyl cellulose and so on; the sustained-release microspheres can further be made into a sustained-release implant which is injected or arranged in a tumor or the tumor periphery, and the local drug release can approximately last 30 to 50 days. The independent application of the sustained-release injection and the sustained-release implant can effectively inhibit the tumor growth, and the combined application with chemotherapy drugs and/or radiotherapy and other non-surgical therapies, and also can significantly enhance the efficacy.
WO2009017795A1 Indazole compounds for treating inflammatory disorders, demyelinating disorders and cancers Compounds of formula (I) or formula (Ia) and a method of treating a patient suffering from certain inflammatory disorders, demyelinating disorders, FLT3- mediated disorders, CSF-lR-mediated disorders, cancers and leukemias, comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or formula (Ia) or a pharmaceutically acceptable salt thereof. (Ia). Definitions for the variables are provided herein.
CN1781509A Composition of luffa seed oil The luffa seed oil composition includes luffa seed oil, vaseline, menthol, perfume, etc. It can reduce patientí»s pain in short period and has obvious curative effect and wide application, owing to its functions of dispelling wind and cold, stopping pain, diminishing inflammation, killing pathogen, stopping itch, expelling toxin, promoting granulation and promoting blood circulation to disperse blood clots.
US6953788 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase The present invention relates to certain novel 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.
CN103550274A Oral medicinal preparation The invention discloses an oral medicinal preparation, and belongs to the technical field of medicines. The medicinal preparation is prepared through main materials and auxiliary materials and prepared into one of buccal tablet, chewable tablet, adhesive tablet and oral pellicle, wherein the main materials include fulvic acid, stevia rebaudiana and sodium chloride. According to the oral medicinal preparation, the local oral medicinal preparation is adopted, so that the shortcomings of slow action and high side effect of systemic administration can be overcome. The medicinal preparation can accelerate the healing of dental ulcer during treating common oral diseases, effectively resists ozostomia caused by the common oral pathogenic bacterium, has a good effect on treating gingivitis and other oral diseases, is fast in action, free of side effect and of high value in clinical health care, and also brings a new choice for clinical medicines.
CN101468164B External targeted transdermal alkalescent blood-regulating agent and preparation method thereof The present invention discloses an external targeted transdermal alkalescent blood adjusting agent and a preparing method thereof, which belongs to a medicine preparation which is characterized by sheet-shaped base material. The blood adjusting agent is prepared by the raw materials of onion extract, folium ginkgo extract, sudroma, wheat germ extract, hexosamine, zinc citrate dehydrate, calcium acetate, lycopin, etc. through the steps of extracting by alcohol, filtering, distilling, condensing, spray drying, and grinding the gel to paste after adding transdermal promoter and medical pressure-sensitive adhesive. The blood adjusting agent can be respectively prepared to patch, membrane agent or gelling agent according to the requirement of dosage form. According to the invention, the medicine is transdermal and enters the blood circulation directly. The blood acid can be quickly and effectively neutralized for remarkably reducing the blood acid. The tedious metabolism routing of oral medicine in vivo is prevented. The transdermal absorption causes that Ca, Zn and other alikaline matter directly and quickly enter to the blood stream for regulating the acid-alkali degree of blood.
US20050203065 Use of A2b adenosine receptor antagonists such as 3-[4-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-bicyclo[2.2.2]oct-1-yl]-propionic acid (BG 9928) Methods useful for preventing, limiting, or treating ischemia reperfusion injury in a mammal are disclosed. More particularly, this invention relates to administering A2b adenosine receptor antagonists to prevent, limit or treat ischemia reperfusion injury.
WO2014020405A1 Cyclic urea- or lactam-substituted quinoxaline-type piperidine compounds and the uses thereof The disclosure relates to Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein R1, R2, Qa, Y1, Z, A, B, Qx, E, G, J, M, U, W, and a are as defined herein, compositions comprising an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxal ine-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound.
CN103239411A Cefdinir, citric acid and sodium citrate dry suspension composition The invention provides a cefdinir (C14H13N5O5S2), citric acid and sodium citrate dry suspension composition and a preparation method thereof. The cefdinir, citric acid and sodium citrate dry suspension composition comprises the following components in parts by weight: 100 parts of cefdinir, 1900-2100 parts of a diluent, 120-200 parts of a flocculant, 28-35 parts of a corrigent, 185-195 parts of an adhesive, 15-30 parts of a suspending aid, 8-12 parts of a flow aid and 1.5-2.5 parts of a lubricant. The cefdinir, citric acid and sodium citrate dry suspension composition disclosed by the invention is convenient for being taken by patients, and has high bioavailability and stability.
WO2012162629A2 Popcorn shape gold nanoparticle for targeted diagnosis, photothermal treatment and in-situ monitoring therapy response for cancer and multiple drug resistance bacteria The present invention provides multifunctional popcorn- shaped gold nanomaterial for sensing, treatment and for a unique way of monitoring treatment effectiveness during therapy process of different human cancer cells and pathogenic bacteria. It consists of the following steps 1) Synthesis of popcorn- shaped gold nanoparticles of different sizes. 2) Design of multifunctional popcorn-shaped gold nanoparticle for targeted sensing, therapy and monitoring therapy effectiveness for different human cancer cells (liver, breast, skin and prostate) and drug resistance bacteria. 3) Design of portable SERS sensor for cancer detection, treatment and for monitoring treatment effectiveness using the same instrument, and 4) Application of our approach to detect and kill MDRB from food sample.
US20090270347 Methods of producing microparticles Methods of producing microparticles, and especially chitin microparticles (CMP), are disclosed that involve reducing the size of (larger) particles using a (high shear) microfluidising instrument.
CN101390844B Arginine ibuprofen tablet and preparation method thereof The invention relates to an arginine ibuprofen tablet which is antipyretic and analgesic, and a preparation method. The arginine ibuprofen tablet contains arginine ibuprofen and auxiliary material by weight proportion: 30%-90% of arginine ibuprofen, 10%-70% of auxiliary material and 0-10% of coating material. The preparation method adopts raw material direction compression or granule preparation;the prepared tablet can be coated or not be coated. The arginine ibuprofen tablet has short response time. As indicated in dissolution test, the dissolution rate is more than 95% in 20 minutes. 20 male volunteers take two preparations of arginine ibuprofen tablets (equal to 400 mg of ibuprofen) and ibuprofen tablets (400mg) for relative bioavailability research; the peak time of arginine ibuprofen tablet is 0.5h and the peak time of ibuprofen tablet is 2.0h. The test indicates that the arginine ibuprofen tablet has quick absorption and short peak time. Besides, the arginine ibuprofen tablet overcomes the pungent taste of arginine ibuprofen syrup and granules and can be taken by patients conveniently, so as to have the advantages of convenient carrying and low cost.
US7235550 Polycyclic azaindole compounds The invention relates to compounds of formula (I): wherein: G1 represents an alkylene chain as defined in the description, A represents R2 and R3 represent hydrogen, alkyl, alkoxy or hydroxy or together form oxo, R4 and R5 represent hydrogen, R1 is as defined in the description, and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.
US20110008325 Inhalant Formulation Containing Sulfoalkyl Ether Cyclodextrin and Corticosteroid Prepared from a Unit Dose Suspension An inhalable unit dose liquid formulation containing SAE-CD and corticosteroid is provided. The formulation is adapted for administration to a subject by nebulization with any known nebulizer. The formulation can be included in a kit. The formulation is administered as an aqueous solution or concentrated composition. The formulation is employed in an improved nebulization system for administering corticosteroid by inhalation. SAE-CD present in the formulation significantly enhances the chemical stability of corticosteroid, such as budesonide. A method of administering the formulation by inhalation is provided. The formulation can also be administered by conventional nasal delivery apparatus. The formulation is prepared by mixing SAE-CD, in solid or liquid (dissolved) form, with an inhalable suspension-based unit dose formulation.
WO2008034781A1 Cysteine protease inhibitor salt The compound N-[(S)-1 -((3aS,6S,6aS)-6-fluoro-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)- 3-methyl-butyl]-4-[2-(4-methyl-piperazin-1 -yl)-thiazol-4-yl]-benzamide benzenesulphonate, its use as a medicament and methods of preparation.
US20120244172 Conjudates of Pyrrolo[1,4]Benzodiazepine Dimers As Anticancer Agents The present invention relates to pyrrolo[1,4]benzodiazepine (PBD) dimer conjugates, to the compositions comprising them and to their therapeutic application, in particular as anticancer agents. The invention also relates to the process for the preparation of the conjugates, to their application as anticancer agents and to the dimers themselves.
CN101284126A Attapulgite kibe chrisma The invention discloses an attapulgite chilblain ointment, which is prepared from purified attapulgite clay, vaseline, alcohol extractive solution of red pepper, alcohol extractive solution of safflower, alcohol extractive solution of purple garlic, alcohol extractive solution of ginger, alcohol extractive solution of pricklyash peel, alcohol extractive solution of notoginseng, alcohol extractive solution of borneol, and honey by mixing, stirring at a high speed to obtain paste, vacuum degassing and canning. The chilblain ointment employs purified attapulgite clay as binder in combination with vaseline to increase chilblain preparation adhesion, and improve pharmaceutical usage effect; and has no greasy feeling and easy cleaning. The chilblain ointment has the effects of promoting the flow of qi by warming the channel, promoting blood circulation, decreasing swelling, inhibiting inflammation, relieving pain, and abating skin pruritus; and can be used for preventing and treating slight chilblain.
WO2013100459A1 Composition comprising hair telogen- or catagen-inducing agent for preventing and alleviating alopecia caused by anticancer therapy Disclosed is a pharmaceutical composition comprising one or more hair telogen- and/or catagen-inducing agents for preventing and alleviating alopecia caused by anticancer chemotherapy and radiotherapy. Also disclosed is a method for preventing and alleviating alopecia caused by anticancer chemotherapy and radiotherapy, said method comprising a step of topically administrating one or more hair anagen- and/or catagen-inducing agents into the scalp of a patient in an effective dosage for prevention, alleviation or treatment. Further disclosed is a method for preventing and alleviating alopecia due to anticancer chemotherapy and radiotherapy by inducing a hair growth cycle through anagen and/or catagen. The composition and method according to the present invention can reduce dystrophy of hair caused by anticancer chemotherapy and radiotherapy to thereby reduce alopecia which is a side effect, and also facilitate the primary recovery of hair after alopecia. Therefore, the composition of the present invention can maximize therapeutic effects by preventing and/or repressing alopecia caused by side effects, when used together with cancer therapy to improve the quality of life of patients and encourage patients to actively participate in cancer therapy.
CN103130680A High-optical-purity alkannin and Akannin naphthazarin nuclear parent hydroxyl methylation carbonyl oxime derivative and preparation method and application thereof The invention discloses a high-optical-purity aklannin and Alkannin naphthazarin nuclear parent hydroxyl methylation carbonyl oxime derivative and a preparation method and application of the high-optical-purity aklannin and Alkannin naphthazarin nuclear parent hydroxyl methylation carbonyl oxime derivative. The structural formula of the derivative is shown in (I), (II), and (IIi) or (IV), wherein R1 is alkane, olefin and arene or substituting arene, or H, wherein the each of the alkane, the olefin and the arene or the substituting arene comprises 1-6 carbon atoms, and R2 is alkane, olefin and arene or substituting arene, or H, wherein each of the alkane, the olefin and the arene or the substituting arene comprises 1-6 carbon atoms. The high-optical-purity aklannin and Alkannin naphthazarin nuclear parent hydroxyl methylation carbonyl oxime derivative is high in optical purity, and novel in structure. Pharmacology experiments prove that compounds of the type have antineoplastic activity, and compared with aklannin and Alkannin which are parent compounds of the compounds, the compounds are equal to or stronger than the parent compounds in activity, and can be applied to preparation of antineoplastic drugs.
US20080103210 wide spectrum disinfectant The invention discloses methods of making and uses for wide spectrum disinfectants including as components an alcohol, O-phenylphenol, chlorhexidine gluconate, nonoxynol-9, benzalkonium chloride, and deionized double distilled water wherein on a weight/volume ratio the alcohol comprises from 50% to 80%, the O-phenylphenol comprises from 0.1% to 0.8%, the chlorhexidine gluconate comprises from 0.1% to 1%, the nonoxynol-9 comprises from 0.02% to 1%, and the benzalkonium chloride comprises from 0.15% to 1%.
CN103623007A Externally-applied ointment for treating ringworm of scalp and preparation and application methods thereof The invention discloses an externally-applied ointment for treating ringworm of scalp. The externally-applied ointment comprises the following components by weight percent: 8-15% of iodine, 30-40% of honey, 40-45% of pearl powder, 1.05-1.58% of table vinegar and 200-400 U/100g of fungicidin. The preparation method of the ointment comprises the following steps: (1) grinding fungicidin into fine powder for later use; (2) mixing and evenly agitating the fungicidin which is ground into fine powder with honey, nano pearl powder, an iodine solution and the table vinegar, storing at the temperature of 4-10 DEG C for at least three days. The application method of the ointment comprises the following steps: taking the ointment which is stored for three days at the temperature of 4-10 DEG C and evenly coating the ointment on the part with the ringworm of the scalp, wherein the drug delivery range exceeds the diseased region 1-2cm, the ointment is coated twice every day, and seven days are taken as a treatment course. The externally-applied ointment is simple in formula, low in price, convenient to use, good for preparation and treatment operation, and reliable in curative effect, and can be self-made no matter in families, clinics or communities; meanwhile, damage and stimulation to the skin caused by other ointments are eliminated. The external ointment is free of toxic and side effects, and good for popularization in hospitals, communities and families, can be used for a long period of time, and has good social and economic benefits.
US7652017 Therapy for central nervous system, brain disorders A therapeutic and/or prophylactic agent for nervous system disorder comprising as the active ingredient substances having an effect of improving calcium ion uptake of cardiac sarcoplasmic reticulum and/or an effect of inhibiting overaccumulation of intracellular calcium ions is offered. Preferably, the therapeutic and/or prophylactic agent for disease selected from the group consisting of cerebrovascular disease, traumatic head injury and postencephalitis and the therapeutic and/or prophylactic agent for disease selected from the group consisting of dementia and neuronal degeneration disease are offered.
CN101987092A Novel pharmaceutical composition containing analgesic The invention discloses a compound slow release preparation prepared from acetaminophen and tramadol hydrochloride for the first time, realizes taking medicine twice per day, and reduces non-indication of patients to the medicine, and the sustained medicine effect can achieve abirritation for a long time.
CN102908336A Stable preparation of phosphatidylserine and preparation method, application as well as application product of stable preparation The invention relates to a stable preparation of phosphatidylserine and a preparation method, application as well as an application product of the stable preparation. The preparation method comprises the following step of processing the phosphatidylserine through microencapsulation, micro-pelletization or liposome encapsulation. The stable preparation of the phosphatidylserine can be independently applied as a medicine or can be added into daily foods, drinks and health-care products, also has an important effect on health care of brains while guaranteeing the color and the taste of the daily foods and the drinks of people and is of great benefit to brain disorder such as nutritional supplement of brain development of students, overstrain of nerves of the adults, and memory loss, brain atrophy and senile dementia of the middle aged and elderly people.
WO2008036022A1 Tetrahydro-lh-pyrido[3,4-b] indole derivatives as cb1 receptor ligands The present invention provides tetrahydro-1H-pyrido [3,4- b] indole derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds act as cannabinoid receptor ligands (CB1) and thus may be used in the treatment of pain, cancer, multiple sclerosis, Parkinson's disease, Huntington's chorea, Alzheimer's disease, anxiety disorders, gastrointestinal disorders and/or cardiovascular disorders.
WO2013019966A1 Aromatic bycyclic derivatives as cxcr4 receptor modulators The present invention relates to novel aromatic bicyclic diamine derivatives, such as 6,7-dihydro-5H-cyclopenta[d]pyrimidine-2,4-diamine or thieno[3,2-d]pyrimidine-2,4-diamine compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the CXCR4 receptor for the treatment of e.g. ocular disorders.
CN103068403A Method and composition for treating, preventing and diagnosing cancer containing cancer stem cells or derived therefrom Provided are a method and a composition for treating, preventing and diagnosing cancer containing cancer stem cells or derived therefrom.
US7547728 (N-(4-nitro-3-trifluoromethyl)phenyl)-(2S)-3-(4- (acetylamino) phenoxy)-2-hydroxy-2-methylpropanamide) derivatives This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide or any combination thereof, as described herein.
CN101524426B Germinal preparation with androgenetic alopecia treatment effect The invention discloses a germinal preparation with androgenetic alopecia treatment effect. The germinal preparation comprises extracting solution of ethanol-water solution of a therapeutically effective amount of coffee, a pharmaceutically acceptable carrier and other active substances. Tests prove that the germinal preparation with androgenetic alopecia treatment effect has significant effect on treating androgenetic alopecia, and has no toxicity and other side effects, active ingredients of the preparation are derived from natural plant compositions, and the germinal preparation has the advantages of simple preparation, easy use, good curative effect and few side effects.
CN103228643A Benzazole derivatives as histamine H4 receptor ligands The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.
CN103570626A Salt of dihydropyrimidine derivative The invention relates to a fumarate or a pharmaceutically acceptable solvate of a dihydropyrimidine derivative, namely 4-(2-chloro-4-fluorophenyl)-6-(morpholin-1-ylmethyl)-2-(2, 4, 6-trifluorophenyl)-1, 4-dihydropyrimidine-5-carboxylic acid ethyl ester, as well as an application thereof in preparation of medicaments for treating hepatitis B.
CN101953836A Application of fluoropirfenidone in preparing medicaments for treating psoriasis The invention relates to new pharmaceutical application of fluoropirfenidone, in particular to the application of fluoropirfenidone in preparing medicaments for treating the psoriasis. When the fluoropirfenidone is used for treating the psoriasis, the fluoropirfenidone is administrated in a local and external form.
CN103263020A Preparation of teenager nutrient supplements A preparation of teenager nutrient supplements is prepared by taking calcium carbonate, calcium gluconate, zinc gluconate, aspartame, magnesium stearate, povidone K30 and starch, finely smashing, sieving with a 100-sieve, weighing a proper amount of the calcium carbonate, the calcium gluconate, the zinc gluconate, an orange-flavour essence, the aspartame, vitamin D3 and the starch, mixing, uniformly stirring, adding a proper amount of the povidone K30 for several times, fully mixing, preparing into particles by a dry method, granulating; taking a proper amount of the magnesium stearate, adding into the above particle mixture, uniformly mixing, tabletting, and packaging into the finish product. The supplements provided by the invention can be used as calcium-zinc nutrient supplements and applied for teenagers.
WO2008146167A3 Improved methods of using phosphoantigens together with interleukin-2 for the treatment of cancer The present invention therefore provides novel approaches and strategies for efficient regulation of γδ T cells in vivo, in a subject, particularly a human subject or a non-human primate. The present invention now discloses particular compositions and methods that can be used to induce the proliferation of γδ T cells in vivo, in a subject. These compositions and methods employ the conjoint treatment of an individual with a γδ T cell activating compound and IL-2 and are particularly suited for immunotherapy in a subject, particularly in a subject having a cancer or an infectious disease.
WO2007123516A1 C-fms kinase inhibitors The invention is directed to compounds of Formula II: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
WO2007026203A1 A pharmaceutical composition comprising mahanine useful for the treatment of prostate cancer The present invention relates to an herbal extract obtained from the leaves or any other plant part of Murrya koenigii useful for the treatment of prostate cancer in a subject.
US20100144663 2, 6-Dinitrogen-Containing Substituted Purine Derivatives, The Preparation And Uses Thereof The present invention provides 2,6-dinitrogen-containing substituted purine compounds of formula (A) or salts or solvates thereof or the solvates of salts thereof, as well as pharmaceutical compositions containing such compounds. The compounds of the present invention have the characteristics of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds.
US20080139504 Method for Improving the Fertility of Animals This invention is in the field of animal food, in particular food for female animals in their reproductive phase. Food according to the invention improves the fertility of animals and increases their chances on a pregnancy. It was found that the fertility of animals may be improved by feeding the animal with a certain amount of naturally occurring immune enhancing ingredients such as beta-glucans and/or phytohormones like auxin or gibberellic acid. Also, combinations of these substances, in particular the combination of beta-glucans and phytohormones, were shown to have a synergistic effect in that they improved the fertility of the animal more than these individual components on their own.
CN1969865A Method for preparing colon targeted pill of doxycycline used for poultry and livestock The invention relates to Doxycycline colon-targeting pills which comprise Doxycycline as the main ingredient, and blank pellets are employed. The medicinal layer comprises Doxycycline, 8% retarding layer of hexadecyl alcohol, 2% retarding layer of HPMC, 15% pH responsive film of acrylic resin S100. The prepared colon-targeting pills are of retarding-and-pH responsive combined type which can achieve the positioned medicinal release on the animal's colons, the curative effects for localized infection and general infection can be improved substantially.
US20090325868 Materials And Methods For FOXP3 Tumor Suppression Provided herein are methods of treating a cancer in a subject comprising administering a FOXP3 protein, a nucleic acid encoding a FOXP3 protein, or an inducing compound which induces FOXP3 protein expression. Methods of altering a phenotype of a cancer cell or tumor cell, methods of inhibiting growth of such cells, and methods of inducing apoptosis of these cells are also provided herein. These methods comprise contacting the cell with a FOXP3 protein, a nucleic acid encoding a FOXP3 protein, or an inducing compound which induces FOXP3 protein expression. Further provided herein are diagnostic methods, comprising comparing the expression or structure of a FOXP3 protein or FOXP3 gene in a test sample to that of a normal or prior sample. A method of screening a test compound for anti-cancer activity comprising administering to cells the test compound and measuring FOXP3 protein or FOXP3 gene expression is moreover provided herein.
CN101229179B Use of oil orange phlorizin-B in preparing medicine The invention provides a medical combination with active component of sesquiterpenes composition Phyllaemblinin B; the composition can be extracted and separated from emblic leafflower fruit, the medical plants of genus Phyllanthus; the invention also provides an application of active component of the medicine in preparation of anti-coxsackie virus B3 medicines and an application in preparation ofmedicines for treating viral myocarditis.
CN101416953A Tacrolimus soft capsules and preparation method thereof The invention discloses a tacrolimus soft capsule which consists of a capsule body and contents in the capsule body, wherein, the ingredients of the contents comprise tacrolimus, PEG400, hydroxypropyl-beta-cyclodextrin and glycerin; the ingredients of the capsule body comprise gross rubber, a plasticizer, water, a preservative, a pigment and a screening agent; the preparation method of the capsule comprises the following steps: stirring and dissolving the tacrolimus, the PEG400, the hydroxypropyl-beta-cyclodextrin and the glycerin to prepare a solution of the contents, putting the plasticizer, the gross rubber and the water into a glue cooker, then evenly blending the mixture till the mixture is dissolved into a rubber solution, adding the pigment, the screening agent and the preservative into the rubber solution and then stirring manually till the color of the rubber solution becomes even, degassing the rubber solution in vacuum to obtain a glue solution, pressing the obtained solution of the contents and the glue solution into soft capsules by a revolving block press, washing oil coatings on the surfaces of the soft capsules by using 95 percent of ethanol, and carrying out pneumatic drying at the temperature of 25 DEG C to 28DEG C to obtain the finished products of the soft capsules. The tacrolimus soft capsule has high bioavailability, contains no organic solvents and has no toxic and side effects on human bodies.
CN101890108A Prescription and preparation method of mixture for relieving pain and arresting diarrhea The invention relates to a mixture for relieving pain and arresting diarrhea. A preparation with the effects of relieving spasm and pain and arresting diarrhea is prepared by compounding procaine hydrochloride, tinctura belladonnae, compound camphor tincture and the like. The preparation has the effects of relieving the pain of the spasm of smooth muscles of the gastrointestinal tract, and inhibiting glandular secretion to arrest diarrhea at the same time. The preparation has good effect of treating abdominal pain and diarrhea caused by acute and chronic gastroenteritis and gastroduodenal ulcer through synergy and is suitable for adults and children.
CN102973503A Norcantharidin derivative lipid microsphere injection and preparation method thereof The invention relates to norcantharidin derivative lipid microsphere injection and a preparation method thereof. The injection contains norcantharidin imide derivative, oil phase, water and surfactant; and the formula of the injection contains the following components by mass: 5 to 30 percent of oil phase, 0.001 to 1 percent of norcantharidin imide N-alkyl derivative, 0.5 to 7 percent of surfactant, 1 to 5 percent of osmotic pressure regulator, and the balance of injection water. Norcantharidin is connected with a long-chain saturated alkane group through amino, so that the lipid solubility of the injection is greatly improved, and the lipid solubility of the injection is improved together with increase of the chain length of the saturated alkane group. Lipid microspheres can carry medicaments with the granularity of more than 90 percent into lipid cores and (or) an interfacial film, so that the medicament loading capacity and the encapsulation efficiency are greatly improved, the vascular stimulation during injection is reduced, the physical and chemical stability of the medicaments and the lipid microsphere injection is improved, the in-vivo acting time of the medicaments is prolonged, the treatment effect is improved, and the toxic or side effect is reduced.
CN103588778A Strontium cantharidate and preparation method thereof The invention discloses strontium cantharidate. A structural formula (I) of the strontium cantharidate is as follows. A preparation method of the strontium cantharidate comprises the steps as follows: according to the weight ratio of 1:(30-50), trichloromethane or isopropanol is added into a cantharidin pure product and heated, so that the mixture is dissolved; at the same time, strontium hydroxide is added into isometric distilled water of the trichloromethane or the isopropanol, uniform mixing is performed, and the molar ratio of cantharidin to the strontium hydroxide is in a range of (3:1)-(3:2); a strontium hydroxide solution is added into a trichloromethane solution or an isopropanol solution which dissolves the cantharidin, and magnetic stirring is performed for 6-12 hours; after stirring, the mixture is heated to 60-75 DEG C, and the trichloromethane or the isopropanol is volatilized, so that a white suspension is obtained; the suspension is placed into a drying oven, concentrated and dried, so that white crystal powder is obtained; and according to the weight ratio of (30-50):1, the trichloromethane or the isopropanol is added into the white crystal powder and heated to 40 DEGC, the temperature is kept until the cantharidin is dissolved, then filtering and drying are performed, and white crystal powder is obtained, so that the strontium cantharidate is obtained. The strontium cantharidate and the preparation method thereof have the characteristics as follows: the antitumor activity is higher, the process is simple, the operation is facilitated, the safety is good, the finished product performance is stable, and the purity is high.
WO2013072766A3 Process for cabazitaxel and intermediates thereof The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.
US20090004173 Diagnosis and Treatment of Drug Resistant Leukemia The present invention encompasses methods and compositions useful in the diagnosis and treatment of drug resistant leukemia. The invention provides a number of genes that are differentially expressed between drug resistant and drug sensitive acute lymphoblastic leukemia (ALL). These genes act as biomarkers for drug resistant leukemia, and further serve as molecular targets for drugs useful in treating drug resistant leukemia. Accordingly, the invention provides methods of diagnosing drug resistant leukemia and methods of selecting a therapy for subjects affected by drug-resistant leukemia. The invention also provides methods for screening for compounds for treating drug-resistant leukemia, and improved methods for treating drug-resistant leukemia. Compositions of the invention include arrays, computer readable media, and kits for use in the methods of the invention.
CN102210666A Medical use of salvianolic acid A The invention relates to the technical field of medicines and discloses the new use of salvianolic acid A, in particular the use of salvianolic acid A in the preparation of medicines for increasing cyclic adenosine monophosphate (CAMP) content in soterocyte and/or blood plasma, preparation of medicines for inhibiting activity of phosphodiesterase in soterocyte, preparation of medicines for promoting activity of adenylate activating enzyme and preparation of medicines for inhibiting calcium ion concentration in cytoplasm of soterocyte, in particular preparation of medicines for preventing or treating myocardial ischemia-reperfusion injury caused by thrombolysis, percutaneous coronary intervention, coronary artery bypass surgery and the like.
CN103655507A Moxifloxacin hydrochloride tablet and preparation method thereof The invention relates to the field of pharmacy technologies and in particular relates to a moxifloxacin hydrochloride tablet and a preparation method thereof. The moxifloxacin hydrochloride tablet is prepared from the following raw materials in parts by weight: 60-64 parts of moxifloxacin hydrochloride, 19-26 parts of filler, 7.0-12.5 parts of disintegrating agent, 0.6-1.6 parts of flow aid, 2.5-3.7 parts of adhesive and 1.4-2.6 parts of opadry film coating powder. The preparation method of the moxifloxacin hydrochloride tablet is simple and feasible. Due to the proportional composition of the components of the moxifloxacin hydrochloride tablet and the process, the problem of disintegrating time limit is solved; due to the adoption of the opadry film coating powder, the moxifloxacin hydrochloride tablet is attractive in appearance and the stability of the tablet is ensured; the moxifloxacin hydrochloride tablet is appropriate in hardness, disintegration property, dissolvability and stability; in addition, the auxiliary material used for the moxifloxacin hydrochloride tablet is low in cost, safe and reliable; industrialization and clinical use are facilitated.
WO2011014098A1 Hydrogenated pyrido[4,3-b]indole derivatives, pharmaceutical composition and methods for the production and use thereof The present invention relates to novel physiologically active hydrogenated pyrido[4,3-b]indole derivatives which exhibit neuroprotective and cognitive stimulatory activity attributable to the interaction of the aforesaid substances with 5-HT6 and 5-HT7 serotonin receptors, butyrylcholinesterase inhibition and action on the mitochondria. The invention relates to medicinal substances, pharmaceutical compositions having the novel hydrogenated pyrido[4,3-b]indole derivatives as the base thereof and novel drugs which can be used to treat diseases and conditions of the central nervous system of humans and warm-blooded animals. The invention also relates to the use of the aforementioned substances, compositions and preparations in the field of medicine and can be used in the manufacture of neuropharmacological agents for treating neurodegenerative diseases and restoring memory and other cognitive functions lost as a result of disease, time or adverse effects. The invention can also be used to produce novel "molecular pharmacological instruments" which make it possible to study (in vitro and in vivo) the biochemical signalling systems and neurochemical mechanisms of the central nervous system. The group of claimed compounds includes novel hydrogenated pyrido[4,3-b]indole derivatives substituted at positions 1 and/or 3 of the piperidine fragment, in the form of bases or salts thereof with pharmacologically acceptable acids, as well as in the form of individual optical isomers or blends thereof, represented collectively by the general formula I.
WO2014142092A1 Novel pi polyamide Provided is a medicinal agent which is useful for the prevention or treatment of prostate cancer and is safe and stable. A novel PI polyamide is obtained, which can recognize a nucleotide sequence that occurs in a transcription regulatory domain (an AR responsive domain) in ACSL3 gene and is specific to an Oct1 gene binding sequence capable of regulating the transcriptional activity of AR and can bind to the nucleotide sequence. Thus, also provided are an ACSL3 gene expression inhibitor and a prophylactic and/or therapeutic agent for prostate cancer, each of which contains the PI polyamide as an active ingredient.
US7094774 26,27-homologated-20-epi-2-alkylidene-19-nor-vitamin D compounds This invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 and R8, which may be the same or different, are each selected from hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or when taken together represent the group —(CH2)x— where x is an integer from 2 to 5, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by relatively high intestinal calcium transport activity and relatively high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.
US20080275083 2,3,4,9-tetrahydro-1h-carbazoles The present invention relates to 2,3,4,9-tetrahydro-1H-carbazoles of the general formula I, in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
US20090028791 Dichloroacetate Analogs as Imaging Agents A compound having structure I: wherein xC is selected from the group consisting of 11C, 12C, and 13C; R is selected from the group consisting of —OH, —O−R4+ wherein R4 is selected from the group consisting of Na and K, —OR3 wherein R3 is selected from the group consisting of C1-8 alkyl and C1-8 alkenyl, —NH2, and NHR3; R′ is selected from the group consisting of —H, —Cl, —F, —Br, and —I; R″ is selected from the group consisting of —H, —Cl, —F, —Br, and —I; and R′″ is selected from the group consisting of —H, —Cl, —F, —Br, —I, 18F, 19F, 75Br, 76Br, 77Br, 123I, 124I, and 131I; provided, when xC is 12C, R′″ is selected from the group consisting of 18F, 19F, 75Br, 76Br, 77Br, 123I, 124I, and 131I. Also, a method of imaging in a mammal a medical condition, such as a cancer, lactic acidosis, or cardiac or cardiovascular function by administering to the mammal a composition comprising a compound having structure I and observing the distribution of the compound in the mammal by an imaging modality selected from the group consisting of positron emission tomography (PET) imaging, single photon emission computed tomography (SPECT), gamma camera devices, magnetic resonance imaging (MRI), and hand-held radiation detection probes. In addition, a method of treating a cancer in a mammal by administering to the mammal a composition comprising a compound having structure I.
CN101057831A Docetaxel liposome novel preparations and its preparation method The invention discloses a new dosage form for polyene alcohols Paclitaxel liposome and the preparing method. The invention employs membrane dispersion method, organic solvent injection method to prepare polyene alcohols Paclitaxel liposome or employs PEG modified phosphatide or other liposome material to modify liposome and produce long circulating liposome, then produce polyene alcohols Paclitaxel injection and freeze drying agent through processes of super-sound, squeezing or high-pressure homogeneity. Compared with normal injection, the polyene alcohols Paclitaxel liposome is characterized in that it can reduce medicine toxic effect, the long circulating liposome greatly increases the circulating time of liposome in the body and the medicine can target tumor more effectively.
US20080181868 Macrocylic oximyl hepatitis c protease inhibitors The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
US20110224248 Azaquinolones that inhibit prolyl hydroxylase Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
US20100278829 Dual inhibition of immunophilin/cyclophilin family members and emmprin immunoglobulin receptor superfamily members The present disclosure provides methods and compositions for modulating an adaptive immune response without significantly affecting an innate immunity response in a subject by modulating a combination of an Immunophilin/Cyclophilin Family Member and an EMMPRIN Immunoglobulin Receptor Superfamily Member. The present invention also provides methods and compositions for treating a variety of clinical conditions by modulating an Immunophilin/Cyclophilin Family Member and an EMMPRIN Immunoglobulin Receptor Superfamily Member.
WO2009071576A1 5-aryl-1,3,4-oxadiazole-2-amines as nicotinic acetylcholine receptor agonists The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of neurological, psychiatric disorders and gastrointestinal disorders. wherein R1 and R2 independently represent hydrogen, C1-6 alkyl or C3-6 cycloalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a nitroge containing heterocyclyl group which is unsubstituted or substituted with 1, 2, or 3 substituents selected from methyl or fluoro; Q represents -(CH2)n- wherein n represents 3 or 4; A represents a phenyl ring and B represents a 5 or 6 membered heteroaryl ring or B represents a phenyl ring and A represents a 5 or 6 membered heteroaryl ring; R3 and R4 independently represent C1-6 alkyl, C1-6 alkoxy and halo; t and m independently represent an integer from 0 to 3. Compounds of formula (I) and their pharmaceutically acceptable salts may have affinity for and be agonists at the nicotinic α7 receptor and are believed to be of potential use in the treatment of neurological diseases including Alzheimer's disease.
CN1730665A PI3K enzyme inhibitor quick-speed screening method The invention discloses a method for screening PI3K enzyme inhibitor which comprises, carrying out molecular docking between the destination compound and PI3Kgamma, virtually screening the destination compound, establishing the screening model again for the PI3Ks enzyme inhibitor, determining the inhibition ratio of the destination compound to PI3K enzyme through western print method, carrying out second round biological activity screening to the destination compound, thus obtaining PI3K enzyme inhibitor.
WO2014143672A1 Macrocyclic compounds as irak4 inhibitors for the treatment of inflammatory diseases Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein i.a. Ring A is phenylene or 5- to 6-membered heteroarylene; Ring B is phenylene, 5- to 6-membered heterocycloalkylene or 5- to 6-membered heteroarylen; R4 is absent, heteroarylene, arylene, C1-3 alkylene, or R4 and R3 taken together with the nitrogen to which they are bound form a 3- to 7-membered heterocycloalkyl ring; R5 is absent, C(0)NR51, NR52 or 0; R6 is C2-10 alkylene or alkenylene, wherein one or two of the carbon atoms in the alkylene chain is optionally replaced by an 0, S, SO, SO2 or NR61, and wherein two of the carbon atoms in the alkylene chain are optionally connected by a two or three carbon atom alkylene chain to form a 5- to 7-membered ring; R7 is absent, NR71 or O. The compounds are IRAK4 inhibitors useful for the treatment of inflammatory diseases.
EP2578231A1 Antitumor t cell response enhancer An objective of the present invention is to provide novel therapeutic agents for cancer, which have an excellent antitumor effect in cancer patients by enhancing their immune function. The present inventors discovered that the administration of an IL-6 inhibitor and/or gemcitabine or a salt thereof to tumor-bearing organisms yields an excellent antitumor T cell response-enhancing effect, and completed the present invention. In addition, the present inventors discovered that the T cell response-enhancing effect produces an excellent antitumor effect.
WO2014117176A1 Methods of improving tolerability, pharmacodynamics, and efficacy of b-alanine and use therefor The present invention relates in some aspects to compositions (e.g., pharmaceutical, nutritional compositions, etc.), formulations, and food or beverage products comprising, consisting essentially of, or consisting of (a) β-alanine or a derivative of β-alanine, and (b) at least one agent that inhibits the N-methyl D- aspartate (NMDA) pathway or a pathway which converges downstream with the NMDA pathway. The compositions, formulations, and food or beverage products are useful for enhancing physical performance, reducing β-alanine- induced paraesthesia, and improving tolerance and compliance to higher doses of β-alanine, thereby reducing the length of time it takes to achieve peak effect of β- alanine, and increasing the magnitude of peak effect on physical performance in a human or animal.
WO2012026906A1 New tiotropium bromide crystal and its production method The present invention relates to a new crystalline form of (1α, 2β, 4β, 5α, 7β)-7-[(hydroxidi-2- thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-bromide and a new method for production of said crystalline form.
WO2008108286A1 Medicinal composition for transdermal absorption, medicinal composition storing unit and transdermal absorption preparation using the same It is intended to provide a transdermal absorption preparation capable of sustaining the blood morphine concentration at the effective level over at least 48 hours, etc. This transdermal absorption preparation comprises a medicinal composition for transdermal absorption in which an active ingredient selected from among morphine and salts thereof is blended in such an amount as corresponding to the saturation solubility or more with an active ingredient-holding vehicle having fluidity at a temperature around the human skin surface temperature and at least a portion of the active ingredient is held as crystals, characterized in that, in the case where a preparation obtained from the above-described medicinal composition for transdermal absorption is applied to the uninjured back of a white rabbit having been shaven with electrical clippers for 72 hours, the available dose of the active ingredient per single dose of the preparation is from 10 mg to 400 mg in terms of morphine base, and the plasma concentrations of the active ingredient 24 hours and 48 hours after the application of the preparation under the above-described conditions are each at least 40 ng/mL in terms of morphine base, and so on.
WO2007087026A3 Solid-state form of amg 706 and pharmaceutical compositions thereof The present invention relates to the compound AMG 706, of formula (I) and in particular to solid-state forms of that drug, to pharmaceutical compositions comprising such solid-state forms, and to processes for preparing them.
CN101288656A Spironolactone sustained-release drop pills and preparation method thereof The invention relates to a drug combination for treating edematous diseases and cardio-cerebrovascular diseases, that is, a spironolactone sustained-release pill and a preparation method thereof; the invention aims at overcoming the defect of the prior art and providing a spironolactone sustained-release pill which is characterized by high drug-loading rate, rapid effect, high bioavailability, controllable drug release, long acting time, less times of medicine taking, less toxic and side effect, low price, convenient oral application and no pollution in the production for patients and medical staffs. The spironolactone sustained-release pill uses spironolactone as raw material and is prepared together with an officinal carrier which takes a hydrophilic framework material and a hydrophobic framework material as substrate.
US20100291181 Therapeutic devices for patterned cell growth The invention provides therapeutic devices comprising a polymeric anti-inflammatory agent that biodegrades to release anti-inflammatory agents. The therapeutic devices are useful for repair and regeneration of a variety of injured tissues.
US20110190330 Spirocyclic gpr40 modulators The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I′A or I′B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
WO2009120371A2 Computationally designed inhibitors of amyloidosis Embodiments of the present invention include methods and systems for designing inhibitors of amyloidosis in humans, domesticated animals, and wild animals as well as inhibitors of amyloidosis designed by the methods and systems. Methods and systems for designing inhibitors of amyloidosis are largely computational, in nature, and are directed to designing various types of polymers, small-molecule organic compounds, organometallic compounds, or non-chemical physical processes that can target the extended-a-strand and a-sheet regions of amyloidogenic protein and polypeptide intermediates in order to prevent aggregation of those intermediates into protofibrils and fibrils that, in turn, recruit additional native-conformation proteins and polypeptides into amyloidogenic intermediates and that additionally aggregate to form higher-order structures, such as plaques observed in the brains of patients suffering from the various spongiform encephalopathies.
WO2009124458A1 Phenylcyclobutylamide derivatives and their stereoisomers, the preparing processes and the uses thereof Phenylcyclobutylamide derivatives and their optical isomers, the preparing processes and the uses thereof, which including the compounds of formula (I), their pure stereoisomers and their pharmaceutically acceptable salts. In formula (I), R is H, formacyl, acetyl, haloacetyl, benzoyl, benzyloxy carbonyl(Cbz), t-butoxy carbonyl(Boc), or 9- fluorenyl methoxyl carbonyl(Fmoc).The present novel compounds have pharmaceutical activity and are prepared by condensation reaction of racemic, levo- or dextro- demethyl Sibutramine and racemic or D/L isoleucine under a mild condition. It is demonstrated that the present compounds have effect of losing weight to obese mode rats in different level and the effect is better than Sibutramine by the animal experiments. So the medicaments prepared by the present compounds or the medicaments prepared by the compositions of the present compounds and other pharmaceutical activity compounds may be used for treating obesity.
WO2005123064A1 Adrenergic complement inhaler comprising compounds such as ascorbates tocopherols or polycaboxylic acid chelators Pharmaceutical compositions consisting essentially of: (a) an adrenergic complement; and (b) a pharmaceutically-acceptable carrier suitable for respiratory administration. Adrenergic complements include ascorbates, tocopherols, and polycarboxylic acid chelators. Methods are also provided for the treatment of respiratory disorders, particularly asthma.
US20090029986 such as 1-{(S)-2-[(5-Bromo-pyrimidin-2-ylamino)-methyl]-piperidin-1-yl}-1-quinolin-2-yl-methanone, used as human orexin receptor antagonist, for the treatment of obesity and insomnia Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.
US8158651 Fentanyl composition for nasal administration The treatment of acute pain with a sufficient dosage by intranasal administration of fentanyl results in a time to onset of action comparable to intravenous administration and a significantly faster onset of action than nasal titration of fentanyl. The nasal administration of a sufficient amount of fentanyl to obtain pain relief has lower maximum plasma concentrations comparable to intravenous administration and results in lower rates of adverse events like respiratory depression, nausea and vomiting. Compositions fur use in the method are also disclosed.
WO2008150190A1 Compositions based on 2,6-di-tert-buthyl-4-methylphenol and a method for treating firearm wounds with the aid of said compositions The invention relates to medicine and pharmacology, in particular to medicinal agents and to a method for accelerated healing firearm wounds by using compositions based on 2,6-di-tert-buthyl-4-methylphenol. The inventive gel based-composition used for treating firearm wounds comprises 5-10 mass% 2,6-di-tert-buthyl-4-methylphenol and 3-5 mass% carnosine in the form of active components. The second inventive gel-based composition comprises 3-5 mass% molluscum instead of carnosine. A gel-based composition used for healing firearm wounds, comprising 5-10 mass% 2,6-di-tert-buthyl-4-methylphenol, 1-3 mass% T-activine and 1-3 mass% tomicidine, is also disclosed. The inventive method for treating firearm wounds, by applying an agent which contains the effective quantity of one of the inventive compositions to a wound, consists in using said agent not later that in 12 hours after injury and, afterwards, in applying it each 1-2 days. The inventive method for treating firearm wounds makes it possible, due to the combined action of the active compounds contained in the inventive compositions, to substantially reduce the size of a lesion area and to accelerate reparative processes, thereby reducing healing time.
CA2665392A1 Anticoagulant compounds The present invention is concerned with anticoagulants (i.e. substances that stop blood from clotting). More specifically, the present invention is concerned with orally available antithrombic oligosaccharides.
CN101574340B Rhododendrin and application of rhododendrin and salts thereof in preparing anti-tumor medicament The invention relates to a new application of rhododendrin and salts thereof, in particular to the application of the rhododendrin and the salts thereof in preparing anti-tumor medicament. According to the results of in vitro cell tests, the invention shows an obvious inhibiting effect against the multiplication of a plurality of tumor cells, is capable of irreversibly inhibiting malignant tumor cells from a plurality of tissues, has relatively little influence on normal human cells and promotes the multiplication of normal liver cells to a certain extent when the concentration thereof is high. According to the results of mouse transplanted tumor in vivo tests, the rhododendrin has certain therapeutical effect on the mouse transplanted tumors, with an inhibition rate over 30 percent afternormal abdominal administration. In brief, the rhododendrin has good anti-tumor activity, is characterized by low toxicity, small side effects and the like, can be synthesized industrially, is low incost and can be used for preparing anti-tumor clinical drugs in combination with an ordinary pharmaceutical carrier or an excipient, thus providing new methods and means for the clinical treatment oftumors and exploring a new direction for the clinical medication. In addition, the salts of the rhododendrin have the same anti-tumor activity as the rhododendrin.
WO2008078100A2 Tricyclic amine derivatives as protein tyrosine kinase inhibitors The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.
US20130023879 Method for augmenting, reducing, and repairing bone with thermoplastic materials (as amended) A method for augmenting a tissue including introducing into the tissue a first thermoplastic material at a first condition; treating the first thermoplastic material to achieve a second condition that includes an at least partially crystalline skin; and introducing a second material into the tissue whereby the first thermoplastic material and the second material are contained by the at least partially crystalline skin. Also a method of fracture reduction in a tissue including exposing to gamma radiation a mass of polycaprolactone characterized by a first shape; heating the mass of irradiated polycaprolactone above its melting temperature; introducing the heated mass of polycaprolactone into the tissue annulus to deform it from the first shape; allowing the material to return to the first shape.
CA2348890C Use of staurosporine derivatives for treating ocular neovascular diseases The invention provides a method for treating or preventing ocular neovascularization. The method administers an effective amount of a staurosporine derivative to treat or prevent retinal or choroidal neovascularization.
US20050153904 Dialysis method There is provided the use of a low molecular weight thrombin inhibitor for the manufacture of a medicament for the treatment by dialysis, particularly haemodialysis, of a patient in need of such treatment, in which the thrombin inhibitor is provided in the dialysing solution, as well as dialysing solutions and concentrates including low molecular weight thrombin inhibitors, such as melagatran.
EP1925305A1 Ih channel inhibitors for the promotion of wakefulness The present invention relates to the use of an Ih channel inhibitor for the manufacture of a medicament for the promotion of wakefulness in a subject in need thereof, in particular, wherein the subject is suffering from excessive sleepiness which may result from a sleep disorder.
CN101947232B Use of cactus pear fruit polysaccharides in preparation of medicaments or health-care products The invention discloses the use of cactus pear fruit polysaccharides extracted from cactus pear fruit in the preparation of medicaments or health-care products for reducing blood pressure, blood fat, blood sugar and resisting tumors. The cactus pear fruit polysaccharides can control the occurrence and development of hypertension, have an active significance for preventing the occurrence and development of hyperlipidemia and fatty degeneration of liver, have potential applications in the prevention and treatment of diabetes and complications and have certain antitumor effect. Therefore, the invention lays a foundation for the development of medicaments or health-care products for preventing and treating hypertension, hyperlipaemia and diabetes and resisting tumors, and promotes the full use of the cactus pear fruit polysaccharides effectively. The cactus pear fruit is a natural plant resource with remarkable medicinal and health-care effects as well as regulation and protection effectson human organs and systems. The price of the cactus pear fruit is relatively low, and the side effects of the cactus pear fruit are relatively fewer. Thus, the cactus pear fruit polysaccharides havegood application prospect in the preparation of the medicaments or health-care products for reducing blood pressure, blood fat, blood sugar and resisting tumors.
CN201238665Y Medical therapy shoes The utility model relates to a pair of curative treatment shoes, for each shoe, an insole is provided with a sunken groove and containers with arbitrary numbers and specifications. The lower end of the container is provided with a container collet, combinations of pulvis medical powder, liquid medical powder and volatile oil are filled in the container, the medical effect of the combinations can be absorbed through the skin of the foot to play the roles of curative treatment and health care of coronary circulation promotion, cell vibrancy, blood circulation acceleration and micro-circulation patency and copiousness. The utility model is suitable for ischemic chronic diseases of diabetes, complications of diabetes, hypertension, coronary heart disease, bradycardia, cerebral infarction, cerebral thrombosis, cerebral haemorrhage sequelae, cervical spondylosis, lumbar vertebra disease, scapulohumeral periarthritis, rheumatism, rheumatoid diseases, gout, caput femoris necrosis, lumbar leg asthenia, insomnia, astriction, prostatoplasia, bronchitis, allelgic asthma, allergic rhinitis, neurodermitis, eczema, drug rash, anaemia, gastricism, enteritis, renal diseases, gynae diseases and the like, can cure a plurality of diseases at the same time, has high remedy rate, safety and practicality, and is simple and easy.
CN101926781A Solid medicinal composition of oxapium iodide The invention discloses a solid medicinal composition of oxapium iodide, in which the grain diameter of an active component is controlled to be less than 30 mu m; and the solid medicinal composition contains a surfactant, has high dissolution rate and favorable absorbility and is used for treating the pains caused by convulsion and motor function disorder symptom.
US20120315223 Compositions for oral use and methods for treating the oral mucosa, lips, and perioral regions Compositions containing polymetal complexes useful in treating disorders of the oral mucosa, lips, and perioral regions are described.
EP2554178A1 Expression modulator for clock gene period The present invention provides a substance which can modulate expression of a Period gene effectively and with a wide range of application. Provided is an expression modulator for the Period gene comprising, as an active ingredient, one or more selected from the group consisting of arnica extract, nuphar extract, black tea extract, Zanthoxylum extract, juniper oil, cedar oil, lavender oil, clove bud oil, cypress oil, rose oil, ylang-ylang oil, galbanum oil, petitgrain oil, pepper oil, thyme oil, basil oil, and beta-caryophyllene.
US7935729 Use of triglyceride oils containing γ-linolenic acid residues and linoleic acid residues for the treatment of neurodegenerative disease Method for treating a patient in need of therapy for a neurodegenerative disease by administering to that patient a therapeutically effective dose of a triglyceride oil containing both γ-linolenic acid and linolenic acid residues as triglyceride ester. The ratio of γ-linolenic acid to linolenic acid residues at the sn-2 position of the triglyceride is at least 0.8. The amount of γ-linolenic acid residues at the sn-2 position is at least 18%. The oil is administered at a dose sufficient to maintain or elevate TGF-β1 levels in the patient at a therapeutic level.
CN103494787A Tamoxifen citrate dropping pill The invention relates to a dropping pill, and particularly relates to a slow-release dropping pill containing tamoxifen citrate clathrates. The tamoxifen citrate is a clathrate with alpha-cyclodextrin as a clathration material, and the weight ratio of tamoxifen citrate to the clathration material is 1:2; the slow-release dropping pill comprises tamoxifen citrate clathrates, a mixture of poloxamer, polyethylene glycol 800, and stearic acid, and a composition of sodium hydrosulphite and sodium phosphate; the condensate liquid is dimethicone.
US7462712 reacting keto ester corresponding compound with phosphorohalide in presence of basic catalyst The present invention relates to an improved process for the preparation of imipenem comprising reacting a bicyclo ketone precursor of the Formula II, wherein R is a protecting group, with a phosphorohalidate in the presence of a base and a catalytic amount of dialkylaminopyridine.
WO2005053648A1 Pre-metered dry powder inhaler for moisture-sensitive medicaments The invention is directed to a pre-metered dry powder inhaler provided with a dry powder dose of tiotropium and excipient(s) loaded into a container comprising a dry, high barrier seal, which prevents ingress of moisture so that the fine particle structure of the powder dose is preserved. The dry powder dose has been formed by either volumetric or electric field dose forming methods. The invention is also directed to a dry powder dose of tiotropium loaded into a container as described above. The dry powder inhaler and the dry powder dose of the invention is intended for use in the treatment of asthma and other respiratory disorders.
WO2013167996A1 Compositions and methods for the treatment of metabolic syndrome The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for the treatment of metabolic syndrome may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of hyperuricemia, gout; dyslipidemia, obesity, urea cycle disorders, hyperglycemia, insulin resistance, diabetes mellitus, diabetes insipidus, type 1 diabetes, type 2 diabetes, microvascular complications,.macrovascular complications, lipid disorders, prediabetes., obesity, arrhythmia, myocardial infarction, stroke, neuropathy, renal complications, hypertriglyceridemia, cardiovascular complications, and post prandial hyperglycemia.
CA2537349A1 The claimed invention relates to novel 4-piperidinecarboxamide and the use thereof for the preparation of medicaments against 5-ht2a receptor-related disorders The present invention relates to compounds of Formula (I) wherein R and R~ are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a 5-HT2A receptor-related disorder.
WO2014049296A1 Combination of laropiprant and metronidazole for the treatment of rosacea The invention relates to a pharmaceutical composition, in particular a dermatological composition, comprising laropiprant, an ester or a pharmaceutically acceptable salt thereof and metronidazole or a pharmaceutically acceptable salt thereof, and to the use of same for the treatment of dermatological conditions, in particular rosacea.
US20090010873 Methods of Cell Therapy, Neurogenesis and Oligodendrogenesis A method is provided for inducing and enhancing neurogenesis and/or oligodendrogenesis from endogenous as well as from exogenously administered stem cells, which comprises administering to an individual in need a neuroprotective agent such as a nervous system (NS)-specific antigen, a peptide derived therefrom, T cells activated therewith, poly-YE, microglia activated by IFN-γ and/or IL-4 and combinations thereof. The method includes stem cell therapy in combination with the neuroprotective agent.
US20100168053 Oral delivery system for methylcobalamin to treat disorders A method of treating a disorder by lollipop administering methylcobalamin, with or without folinic acid by direct delivery to the trigeminal nerve. The disorders addressed are: a) attention deficit hyperactivity disorder (ADHD); b) anxiety, depression, stress and chronic stress; c) socialization problems, mood problems, behavior problems, memory problems; d) dyslexia, depth perception problems, color viewing problems, visual and auditory processing problems, light modulation problems, night vision problems; e) speech problems such as finding words, apraxia, and articulation problems, sleep regulation problems, eye or muscle movement problems; and f) chronic fatigue problems, digestion problems, sensitivity to chemicals, viral infection, inflammatory conditions such as rheumatoid arthritis, sciatica, and fibromyalgia, asthma, irritable bowel, colitis, tinnitus, migraines, nail biting, autoimmune problems. In some embodiments, the disorders that are particularly addressed are ADHD, anxiety, stress and chronic stress, and irritable bowel. A lollipop for treating a psychological or neuro-physiological disorder and method of making thereof.
US20110166149 Pteridine derivatives for treating respiratory disease The invention provides methods and compositions for treating asthma and/or COPD. For example, provided herein are compositions that include a kinase inhibiting agent such as 6,7-bis(3-hydroxyphenyl)-pteridine-2,4-diamine or pharmaceutically acceptable salts thereof; and a surfactant.
EP2675794A1 Selective fak inhibitors A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
CN103113369A Benzo [b][1,8]-naphthyridine-2-(1H)-imide derivative with antitumor activity and synthetic method thereof The invention discloses a novel benzo [b][1, 8]-naphthyridine-2-(1H)-imide derivative which has antitumor activity, and in particular relates to anti-solid tumor activity and more accurately the anti-lung cancer and anti-colon cancer activity as well as a structure shown in formula (I). The invention further discloses a synthetic method. In formula (I), n is 1, 2 or 3, but R, R1, R2, R3 and R4 are defined as in claim 1. The synthetic method comprises the step of heating a 2-halogen-3-formyl quinoline compound with a structure in formula (II) and a compound with a structure in formula (III) in an appropriate solvent in the presence of a catalyst so as to obtain a target product in formula (I).
US7371404 Amphoteric liposomes and their use Amphoteric liposomes are proposed, which comprise positive and negative membrane-based or membrane-forming charge carriers as well as the use of these liposomes.
US7560473 Amine derivative with potassium channel regulatory function, its preparation and use The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression.
EP1517689A2 Selective analgesic agents The invention provides a method for producing a selective analgesic effect outside the brain (e.g. via opioid receptors in the spinal cord) of a mammal, comprising administering to the mammal, an effective analgesic dose of a compound that binds to delta-kappa opioid receptors in the mammal.
CN1650889A Child cough stopping sgrup and its preparation method An infantile anticough syrup for treating infantile cough caused by cold or branchitis is prepared from pentoxyvarine citrate, ammonium chloride, syrup, alcohol solution of nipagin, concentrated mint solution and distilled water through dissolving, filtering, heating, stirring, boiling, cooling and stirring.
US7956045 Improving the health of ruminant animals, increasing milk production in lactating animals, and/or treating and controlling infective diarrhea by the oral administration of an effective amount of an indigestible oligosaccharide of gluco-oligosaccharides and/or isomalto-oligosaccharides; feed additives A method of improving the health and production of ruminant animals, the method including the step of orally administering to the animal an effective amount of an indigestible oligosaccharide selected from the group of gluco-oligosaccharides and isomalto-oligosaccharides.
US20080312217 N,N'-Bis-{4-[N'-(3,5-diamino-6-chloro-pyrazine-2-carbonyl)-guanidino]-butyl}terephthalamide, used for the treatment of conditions mediated by the blockade of an epithelial sodium channels A Compound of formula (I) or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M1, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5, and R5a are as defined herein for the treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergic condition.
WO2009012280A2 Benzimidazole poly(adp-ribose)polymerase inhibitors Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.
EP2167522A2 Triazole-based aminoglycoside-peptide conjugates and methods of use Aminoglycoside-amino acid and -peptide conjugates comprising a triazolyl linker are provided along with efficient methods of their preparation. The aminoglycoside may be an aminoglycoside antibiotic. Conjugates comprising an aminoglycoside antibiotic may exhibit antimicrobial activities against Gram-positive and/or Gram-negative strains and display significantly enhanced activity against multi-drug resistant MRSA and MRSE when compared to their unconjugated aminoglycoside antibiotic counterparts.
EP1485160B1 Intraductal management of breast lesions involving therapeutic or diagnostic agents The present invention relates to an apparatus and method for administering a radioactive tracer dye and an inhibitor compound into a breast duct of the breast and imaging the breast for breast lesions. The radioactive tracer dye may be Tc-99m sestamibi and the inhibitor compound may inhibit a P-glycoprotein pump in tumor cells. When the inhibitor compound inhibits the P-glycoprotein pump in tumor cells, the radioactive tracer dye may effectively accumulate in tumor cells and improve the sensitivity of nuclear imaging of breast lesions.
EP1917248A1 1-acyldihydropyrazol derivatives Compounds of formula (I) in which R1, R2, R3a, R3b, R3c and R3d, which have the meanings cited in Claim 1, are inhibitors of tyrosinkinases, particularly Met kinase and can, among other things, be used for treating tumors.
CA2302496C Urinary incontinence therapy The invention includes a method of treating neurogenic urinary dysfunction that comprises contacting urinary bladder mucosa of a patient afflicted with neurogenic urinary dysfunction with an effective dose of a homovanilloid compound, in particular a compound selected from the group RTX, TYX, 20-homovanilyl-mezerein or 20-homovanillyl-l2-deoxyphorbol-13-phenylacetate. The invention includes treatment of urge incontinence due to detrusor hyperreflexia (DH). The invention also includes treatment of sensory hypersensitivity of the blader resulting from prostate hypertrophy or interstial cystitis, as well as other neurogenic conditions resulting in increased micturition frequency or decreased bladder capacity, with or without frank incontinence.
CN101322686A Daimeton (sodium) suspension injection and preparation thereof The invention relates to a new veterinary medicine preparation (sulfamonomethoxine suspension injection or sulfamonomethoxine sodium suspension injection) and a preparation method thereof; the new veterinary medicine preparation is prepared by taking sulfamonomethoxine or sulfamonomethoxine sodium as main drug and other excipients for assist. The percentage of the main ingredients in the suspension is as follows: 1%-50% (W/V) of sulfamonomethoxine or sulfamonomethoxine sodium and the rest of drug excipients; the excipients include a suspending agent and a disperse medium. The invention takes oil solvent as the disperse medium to prepare sulfamonomethoxine or sulfamonomethoxine sodium into a long-acting and sustained-release preparation; by adopting intramuscular injection for drug administration, the in vivo acting time of the drug can be significantly prolonged, the times of drug administration are reduced and the blood concentration of diseased livestock can keep stable. The new veterinary medicine preparation of the invention is safe, stable, effective and controllable in quality, thus being widely applicable to the treatment of bacterial infection and parasitic infestation in livestock.
WO2012057401A1 Iron oxide nanoparticles in which gluconic acid and non-polymerized biological material are introduced as surface modifier, securing improved biocompatibility by optimum introduction of gluconic acid, and composition for diagnosing and treating cancer, containing same The present invention relates to iron oxide-based nanoparticles comprising: an iron oxide-based central particle; a shell coated with a water-soluble material selected from the group consisting of ATP, NAD, ADP, AMP and NADP which are non-polymerized; and gluconic acid securing binding amounts and binding conditions to ensure the optimum biocompatibility on the surface of the shell, a preparation method thereof, and a contrast medium and a composition for diagnosis and treatment of cancer, containing the same. The iron oxide-based nanoparticles surface-modified with gluconic acid of the present invention reduces a degree removed through uptake by the reticuloendothelial system, thereby improving delivery to a target organ or lesion, and can be used as a contrast medium for diagnosis and treatment capable of simultaneous imaging and treatment.
US20120083470 Inhibitors of tyrosine kinases and uses thereof Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.
CN103497179A Pyrimidine derivatives with benzimidazole structural units as well as preparation method and application thereof The invention belongs to the technical field of chemical synthesis of drugs and discloses a 2-(5H/Cl-benzimidazole-2-dimehtylthio)-4-substituted-6-phenyl pyrimidine derivatives with antitumor activity as well as a synthesis method and application thereof. A series of 6-phenyl-2-thiouracil derivatives with benzimidazole structural units are prepared through reactions such as cyclization, substitution, chlorination, aminolysis and the like by taking ethyl benzoylacetate as the raw material. The compounds provided by the invention have the general formula as shown in a figure I. In-vitro antitumor activity experiments prove that the compounds have remarkable inhibiting and killing effects for various tumor cells.
CN103565764A Mitiglinide calcium composition tablets and preparation method thereof The invention provides mitiglinide calcium composition tablets and a preparation method thereof. The mitiglinide calcium composition tablets comprise the following raw materials in parts by weight: 7-12 parts of mitiglinide calcium, 40-70 parts of lactose, 5-20 parts of pregelatinized starch, 25-60 parts of microcrystalline cellulose, 1-5 parts of hydroxypropyl cellulose, 5-12 parts of silicon dioxide, 0.1-3 parts of magnesium stearate and a proper amount of povidone K30. The mitiglinide calcium composition tablets provided by the invention are easily accessible in raw materials, low in cost, easy to prepare, high in disintegration speed and dissolution rate, good in stability, accurate in dosage and convenient to take and carry; the preparation method is simple in process, easy to control, short in production cycle, low in production cost and suitable for industrial production.
US20100074977 Methods for treating glioblastoma with herbal compositions The inventive subject matter relates to methods for treating glioblastoma, comprising administration of a composition comprising therapeutically effective amounts of supercritical extracts of rosemary, turmeric, oregano and ginger; and therapeutically effective amounts of hydroalcoholic extracts of holy basil, ginger, turmeric, Scutellaria baicalensis, rosemary, green tea, huzhang, Chinese goldthread, and barberry. The inventive subject matter further relates to methods for modulating gene expression of genes selected from the group consisting of interleukin-1α, interleukin-1β, heme oxygenase 1, aldo-keto reductase family 1, member C2, colony stimulating factor 3, leukemia inhibitory factor, heat shock 70 kDa protein, and combinations thereof, by administration of an effective amount of said compositions.
US20100062007 Multi-modal cancer therapy using viral hitch-hiking The present invention relates to an antibody fusion protein which specifically recognizes the VA, HN or F surface antigen of the New Castle Disease Virus (NDV), a surface molecule of a tumor-unspecific T cell or a surface molecule of a dendritic cell and an immunocytokine. Also encompassed by the present invention are polynucleotides encoding the aforementioned antibody fusion protein as well as tumor-unspecific key cells or dendritic cells bound by the antibody fusion protein. Moreover, the present invention relates to a method of treating a tumor in a subject comprising administering to the said subject the antibody fusion protein, the tumor-unspecific T cell, the dendritic cell or the polynucleotide of the invention. Preferably, the said tumor is a solid tumor.
WO2007102368A1 Novel 3-(1-aminoalkylidene)furan-2,4(3h,5h)-dione derivative, method for producing the same, and pharmaceutical composition containing the same as active ingredient Disclosed is a compound which can be used as an active ingredient for an antitumor agent or protein phosphatase inhibitor. Specifically disclosed is a compound represented by the formula (I) below, a salt thereof or a solvate thereof. Also specifically disclosed is a pharmaceutical composition containing such a compound, which has antitumor activity or protein phosphatase inhibitory activity.
US6939542 Contacting vitreous humor with beta-glucuronidase, matrix metalloproteinase, chondroitinase, chondroitin sulfatase, and/or protein kinase; thimerosal-free A thimerosal-free hyaluronidase preparation wherein the preferred hyaluronidase enzyme is devoid of molecular weight fractions below 40,000 MW, between 60-70,000 MW and above 100,000 MW. Also disclosed is a method for accelerating the clearance of hemorrhagic blood from the vitreous humor of the eye, said method comprising the step of contacting at least one hemorrhage-clearing enzyme (e.g., a β-glucuronidase, matrix metalloproteinase, chondroitinase, chondroitin sulfatase or protein kinase) with the vitreous humor in an amount which is effective to cause accelerated clearance of blood therefrom.
WO2006004660A3 Detection of mutations in a gene associated with resistance to viral infection A method for detecting a mutation related to the gene encoding LDLR. This and other disclosed mutations correlate with resistance of humans to viral infection including hepatitis C. Also provided is a therapeutic agent consisting of a protein or polypeptide encoded by the wild-type and mutated genes, or a polynucleotide encoding the protein or polypeptide. Inhibitors of human LDLR, including antisense oligonucleotides, methods, and compositions specific for human LDLR, are also provided.
WO2006101163A1 Medicinal composition for treating/preventing motor organ disease Fullerene inhibits a lowering in the cell proliferation ability of cartilage cells which is observed in treating cultured cartilage cells with cartilage denaturing factors (IL-1β, H2O2). Fullerene inhibits the production of cartilage matrix degenerating enzymes (matrix metalloproteases (MMP)-1, 3 and 13) which is induced in cultured cartilage cells by the cartilage denaturation factors. Fullerene restores a lowering in the cartilage matrix (proteoglycan) synthesis ability which is observed in treating cultured cartilage cells with the cartilage denaturation factors. In an analysis with the use of rabbits suffering from arthritis deformans, the progress of cartilage deformation is relieved by administering fullerene. By adding fullerene to synovial fluid, coefficient of dynamic friction is lowered.
CN101785794B Pharmaceutical composite and application thereof The invention relates to a pharmaceutical composite which contains 20-30 parts of panax notoginseng saponins, 115-125 parts of microcrystalline cellulose, 8-14 parts of hydroxypropyl cellulose, 8-12 parts of sodium carboxymethyl starch and 2-6 parts of aerosol. The pharmaceutical composite can be used to improve the blood indexes.
EP2675460A1 Treatment of submental fat This disclosure relates to compositions, kits and methods for non-surgical reduction of localized subcutaneous fat such as that associated with a cosmetic fat accumulation. The methods employ compositions having specific concentrations of a salt of deoxycholic acid which provides a superior fat cell necrosis with modest adverse effects. Examples of localized subcutaneous fat are found in the submental area, in particular under the chin.
WO2012043680A1 水系皮膚外用剤aqueous topical preparation for use on skin An aqueous topical preparation for use on skin, said preparation containing: water; casein nanoparticles containing a hydroxystilbene such as resveratrol; and a compound that has a thiol group such as cysteine.
CN102234278A (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives, and synthesis method and application thereof The invention discloses (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives, and a synthesis method and application thereof. The structural formula of the compounds is shown as a general formula I. Hexa hydro-pyrazino-pyridino-indoldione compounds are structurally modified by natural amino acid, the water solubility and in-vivo absorption are improved and the anti-thrombotic activity is improved. In-vitro and in-vivo anti-thrombotic activity experiments indicate that the compounds in the general formula I have excellent anti-thrombotic activity, and can be prepared into anti-thrombotic medicines.
EP1443942B1 Pharmaceutical composition for use for the treatment of malignancies comprising in combination a bisphosphonate, a cox-2 inhibitor and a taxol A pharmaceutical composition for treatment of malignancies, in particular a malignant disease which is associated with the development of bone metastases or excessive bone resorption, comprises in combination a bisphosphonates, COX-2 inhibitor and/or a taxol or derivative thereof for simultaneous, sequential or separate use. Also provided is a method of treating a patient suffering from a malignant disease comprising administering to the patient an effective amount of a bisphosphonates, an effective amount of a COX-2 inhibitor and/or and effective amount of a taxol or derivative thereof.
US6878736 Histamine H3 receptor ligands Compounds of formula (I) (and pharmaceutically acceptable salts thereof) are histamine H3 receptor ligands. A in the formula represents (CH2)m, m being from 1 to 3; B is (CH2)n, n being from 1 to 3; x is from 0 to 2; R1 is C1 to C10 hydrocarbyl, in which up to 2 carbon atoms may be replaced by O, S or N; and up to 2 hydrogen atoms may be replaced by halogen; R2 is H or C1 to C15 hydrocarbyl, in which up to 3 carbon atoms may be replaced by O, S or N, and up to 3 hydrogen atoms may be replaced by halogen; R3 is absent when —Y—Z—R2 is attached to W, or is H or C1 to C7 hydrocarbyl when —Y—Z—R2 is not attached to W; W is nitrogen; X is —CH2—, —O— or —NR4—, R4 being H or C1 to C3 alkyl; Y replaces a hydrogen atom on any of A, B, W and X, and is C2 to C10 alkylene, in which one non-terminal carbon atom may be replaced by O; and Z is (II), (III), (IV), (V), (VI), or (VII) wherein R5, R6 and R7 are independently H or C1 to C15 hydrocarbyl, in which up to 3 carbon atoms may be replaced by O or N, and up to 3 hydrogen atoms may be replaced by halogen, and Q is H or methyl, or Q is linked to R5 or R7 to form a five-membered ring or Q is linked to R2 to form a six-membered ring
CN102078323A Minodronate-containing pharmaceutical composition The invention discloses a minodronate-containing pharmaceutical composition, which comprises effective treatment amount of high-nitrogen-containing bisphosphonate compound which are selected from minodronate, medicament stabilizer selected from, e.g. sodium carbonate, and pharmaceutically acceptable auxiliary material which can effectively improve dissolution. The pharmaceutical composition can be used for treating osteoporosis.
US20080299067 Functionalised Siloxanes for Scar Tissue Treatment A novel composition for use in treating a wound, burn or other skin condition comprises one or more compounds of formula (I), wherein: m = 0-6, n = 6-100, Q, R and R′ may be independently selected from, C1-5 alkyl, OU, UOCH2CH3, CH2CH3, UOCH3, OH, O(CH2)y(OU)yCH3, (OCH2CH2)yOU, (OCH2CH2)yOH, UOH, UOU′, UCO2U′, CO2U, UCO2COU, CO2H, UCO2H, COX, UCOX, UCO2 R′, CO2COU, Aryl, ArylU, ArylUU, ArylUU′U″, NH2, UNH2, NHU, NUU′, NO2, UNO2, UCONH2, CONH2, UCONHU′, CONHU, UCONU′U″, CONU′U″, halogen, PO4H3, PO4H3-z, PO4H3-zU (z = 0, 1, 2 or 3), PU3, P U′U″U′″SH, SO2 and SO3H; wherein U, U′, U″ and U′″ may be independently selected from any alkyl, alkenyl or alkynyl group where the number of carbon atoms is between 1 and 31; wherein X=halogen; wherein y=1-100; provided that Q, R and R′ can not all be C1 alkyl; and wherein the compound of formula (I) is present in an amount of at least 1% of the composition.
EP1558600B1 Selected cgrp antagonists, method for production and use thereof as medicament The invention relates to CGRP antagonists of general formula (I), in which A, U, V, W, X and R1 to R 3 are as defined in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures, salts, hydrates of the salts, in particular the physiologically-acceptable salts thereof with inorganic or organic acids, medicaments containing said compounds and the use and methods for production thereof.
US20100124545 Cyclic carboxamide compounds and analogues thereof as of hepatitis c virus The invention provides cyclic carboxamide compounds and analogues thereof of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain cyclic carboxamide compounds and cyclic carboxamide analogues disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more cyclic carboxamide compounds or cyclic carboxamide analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a cyclic carboxamide compound or cyclic carboxamide analogue as the only active agent or may contain a combination of a cyclic carboxamide compound or cyclic carboxamide analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
EP0836476B1 A COSMETIC COMPOSITION comprising the glycopropyl ester of retinoic acid FOR SKIN APPLICATIONS AND PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF skin diseases, TUMOROUS CELLS, BLADDER OR NERVE DISORDERS Compositions based on glyco-alcohol, hydro-alcohol or glyco-hydro-alcohol solutions of a glycol or glyceric ester of retinoic acid, preferably in association with the ethyl ester of retinoic acid and with hydroquinone, have been found to be particularly effective, as such or in cream form, in eliminating unsightly skin disorders such as acne, wrinkles, scars, stretch marks, dark spots, etc., and in treating mycotic skin diseases and psoriasis. Diluted in water, the compositions are also effective in treating falling hair. The basic composition containing the esters of retinoic acid and hydroquinone as an antioxidant may be combined with various known medicinal products, e.g. for enhancing the anti-edema effect of sodium heparin, enhancing the anti-inflammatory effect of niflumic acid, indomethacin and naproxene, and enhancing the antipruritic effect of aqueous extract of tritiam vulgaris.
CN103536618A Ganciclovir composition freeze-dried powder for injection The invention provides a ganciclovir composition freeze-dried powder for injection, and belongs to the field of medicine and medicine preparation technology. The ganciclovir composition freeze-dried powder comprises following raw material ingredients, by weight, 7.26 to 9.17 parts of ganciclovir, 5.15 to 6.56 parts of chitosan nanoparticle, and 80.34 to 87.10 parts of injection water. Advantages of the ganciclovir composition freeze-dried powder are that: 1) toxic effect of the ganciclovir composition freeze-dried powder on cells is reduced; 2) the ganciclovir composition freeze-dried powder is capable of avoiding phagocytosis of mononuclear macrophage on ganciclovir, contact area of ganciclovir with action sites is enlarged, and per unit area medicine concentration is increased; 3) human cytomegalovirus resistance is increased significantly, and medication cycle of patients is shortened, so that occurrence likelihood of adverse drug reaction caused by accumulation of ganciclovir is reduced; 4) no hemolysis, agglutination reaction, stimulus response or anaphylactic reaction is observed in special safety tests such as allergic test, hemolytic test and vascular stimulation test; 5) the chitosan nanoparticle is used as a freeze-dried skeleton agent of the freeze-dried powder injection instead of mannitol, so that active effects of mannitol on human bodies are avoided.
CN103040858A Novel amoxicillin clavulanic acid composition The invention discloses a novel amoxicillin clavulanic acid composition. When pegylation is conducted on the amoxicillin, the medicine water-solubility is improved and at the same time good stability of the medicine is ensured; by modifying the clavulanic acid by using glucuronic acid, the original characteristic of strong hygroscopicity is changed, and problems that the clavulanic acid is poor in mobility, non-uniform when being mixed with the amoxicillin, easy to discolor, deteriorate and degrade and the like caused by the strong hygroscopicity are avoided, so that by carrying out molecular modification on the two active ingredients respectively, not only is the physiochemical property of the medicine changed, but also the stability is greatly improved, the effective content after entering human bodies is ensured, problems that the content is greatly reduced and related substances are increased after an ordinary preparation product in market is prepared into injection are solved, the problem of mass stability of the composition in the production, storage, preparation and injection process is substantially solved, and the use amount of the clavulanic acid is greatly reduced.
US6861436 Useful against multidrug resistant cancer cells Disclosed is a compound represented by Structural Formula (I): Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z1 and Z2 are independently ═O, ═S, ═N—OR12 or ═NR12 R1 and R2 are independently —H, an aliphatic group, a substituted aliphatic group, an unsubstituted non-aromatic heterocylic group, a substituted non-aromatic heterocylic group, an aryl group or a substituted aryl group, provided that R1 and R2 are not both —H. Alternatively, —NR1R2, taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, —C(R4R5)—, —N(R4)—, —O—, —S—, —S(O)—, —S(O)2—, —C(═O)—, —C(═O)—N(R4)—, or —N(R4)—C(═O)—. R4 and R5 are independently —H or a substituted or unsubstituted aliphatic group. R12 is —H or a substituted or unsubstituted alkyl group.
CA2550493A1 Packaging of ferric pyrophosphate for dialysis A stable packaged bicarbonate solution for use in dialysis treatment and for treating anemia, iron deficiency, or reducing the required dose of recombinant erythropoietin to treat anemia includes a bicarbonate solution into which ferric pyrophosphate is dissolved.The amount of ferric pyrophosphate dissolved in the bicarbonate solution is sufficient to provide a therapeutic effect for the treatment of anemia, iron deficiency or to reduce dose of recombinant erythropoietin needed to treat anemia when the bicarbonate solution is combined with other dialysis components to form a dialysate used for dialyzing a patient.The ferric pyrophosphate is stabilized in the bicarbonate solution by holding the solution in a polyolefin container or container liner, such as a high density polyethylene container or liner.
CN101675926A Analgesics and methods of use A method for inducing analgesia and/or inhibiting abuse of abusive substances includes administration of d-methadone metabolites or their structural analogs. The d-methadone metabolites, EMDP and EDDP, and their structural analogs may be incorporated into a suitable pharmaceutical composition for administration to patients. The invention includes the method itself, certain structural analogs, andpharmaceutical compositions for use in accordance with the method.
WO2008150217A1 2-amino-5, 5-diaryl-imidazol-4-one analogs for the inhibition of beta-secretase This invention relates to novel compounds having the structural formula (I) below: formula (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
CN101327307A Medicament for treating cancer and preparation method The invention provides a medicine for remedying cancer, in particular to a medicine for remedying various cancers after surgery. The medicine is characterized in that No. I recipe takes radix rehmanniae, red peony root, bletilla, Szechwan lovage rhizome, wine-madder, salvia, panpax notoginseng, dandelion, APN, rhodiola himalensis, raw radix astragali, angelica, wolfberry fruit, chinese yam, radix pseudostell, membrane of chicken gizzard, asparagus, trichosanthin, hawthorn and so on as raw materials; No. II recipe takes vinegar leaching and frying turtle shell, dried lacquer, duchesnea indica, citrus aurantium, earth frying atractylodes, areca nut, mythic fungus, dodder, sang, raw ochre, pubescent holly, honeysuckleand so on as raw materials; No. III recipe takes sang, liriope, liquorices, cinnamon, herba cistanches, wolfberry fruit and so on as raw materials. The recipes are separately made into decoction in proportion. The medicine uses the comprehensive effect of each medicine to remedy various cancers that have been processed with surgery. The medicine can remove blood heat, influence blood, active blood without randomly influencing, stop blood, eliminate blood stasis, produce new blood and drain deteriorated blood without harm to new blood. The clinical treatment shows that the medicine has significant efficacy.
CN101374522A ANG2 and VEGF inhibitor combinations The invention provides methods for using Ang2 inhibitors in combination with VEGF inhibitors to treat disease. The invention also provides compositions, kits, formulations, and specific disease treatments relating thereto.
CN1680235A Preparation and use of compounds i.e., falcarindiol as inhibitor of protein-tyrosine-phosphatase 1B Production of falcarindiol compound with protein tyrosine phosphatase 1B inhibiting activity extracted, separated and derived from branches and leaves of Aegiceras corniculatum and its use are disclosed. R1, R2 is H, CH3 or Ac in same time. It is carried out by drying and breaking branches and leaves of Aegiceras corniculatum, extracting by alcohol, extracting the subsection by light petroleum, acetic ether and (n-)butanol, silica gel column and Sephadex LH-20 gel column chromatographing the part of acetic ether, separating to obtain monomer compound, analyzing by wave spectrum, determining falcarindiol, acetylating and methylating reacting for falcarindiol, and obtaining acetylate and methylate. It has PTP1B inhibiting activity and can be used for diabetes mellitus and obesity.
US7067511 1,1'-((Propane-1,3-diyl)dioxy)bis((11aS)-7-methoxy-2 -methy lidene-1,2,3,11-tetrahydro-5H-pyrrolo(2,1-c)(1,4)benzodiazep in-5-one) derivatives; viricides, parasiticide, bactericides, gene therapy and treating cisplatin refractory disease Compounds of the formulae Ia and Ib: wherein: A is CH2, or a single bond; R2 is selected from: R, OH, OR, CO2H, CO2R, COH, COR, SO2R, CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn; and R8 is selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn, where R is as defined above, or the compound is a dimer with each monomer being the same or different and being of formula Ia or Ib, where the R8 groups of the monomers form together a bridge having the formula —X—R′—X— linking the monomers, where R′ is an alkylene chain containing from 3 to 12 carbon atoms, which chain may be interrupted by one or more hetero-atoms and/or aromatic rings and may contain one or more carbon-carbon double or triple bonds, and each X is independently selected from O, S, or N; except that in a compound of formula Ia when A is a single bond, then R2 is not CH═CH(CONH2) or CH═CH(CONMe2). Other related compounds are also disclosed.
US20090047368 Polymeric polyphenol extracted from fermented tea, therapeutic agent for mitochondrial disease, preventive/therapeutic agent for diabetes mellitus, and food or beverage [Problem] To provide a new pharmacological action for high-molecular-weight polyphenols [Solution] To provide high-molecular-weight polyphenols extracted from fermented tea (e.g. oolong tea or black tea), which are high-molecular-weight polyphenols with a number average molecular weight ranging from 9,000 to 18,000, and containing in their partial structures a procyanidin structure of polymerized catechins and/or their gallates, and a structure of linkage between the B-rings of catechins and/or their gallates. These high-molecular-weight polyphenols have the functions of mitochondrial activation, suppression of increase in blood glucose, and suppression of weight gain. Therefore, they can be used as drugs for the treatment of mitochondrial disease, and also as drugs for the prevention and treatment of diabetes. They may also be added to health foods and beverages. The selected drawing shows changes in blood glucose level when the said high-molecular-weight polyphenols are given daily to diabetes model mice in specified doses.
EP2617726A1 Diabetes therapeutic agent The problem of the present invention is to provide a compound useful for the prophylaxis or treatment of diseases related to the control of the differentiation of muscle cell or adipocyte differentiation, such as diabetes, obesity, dyslipidemia, and having a superior efficacy. The present invention provides an agent for the prophylaxis or treatment of diabetes, obesity or dyslipidemia, containing a compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a salt thereof or a prodrug thereof.
CN103007222A Foot liquid for treating insomnia The invention discloses a foot liquid for treating insomnia, comprising the following ingredients in parts by weight: 2-8 parts of salvia miltiorrhiza, 8-14 parts of hljmdyz, 10-15 parts of caulis bambusae in taeniam, 6-7 parts of rhizoma atractylodis macrocephalae, 2-8 parts of radix bupleuri, 3-9 parts of magnets, 6-11 parts of rhizoma anemarrhenae, 5-7 parts of platycladi seeds, 2-3 parts of siberian elm bark, 6-12 parts of gingers, 10-18 parts of herba eupatorii, 7-20 parts of purple perilla, 3-5 parts of fructus cnidii and 30-40 parts of water. The foot liquid is convenient to use, plays the role of easing mental anxiety, nourishing liver and kidney, promoting qi circulation to relieve pain, and helping sleeping for enhancing body health, and thoroughly removes insomnia symptoms.
CN103585112A Tamsulosin enteric coated sustained-release pellet and preparation method thereof The invention relates to a tamsulosin enteric coated sustained-release pellet and a preparation method thereof. The tamsulosin enteric coated sustained-release pellet comprises a pellet core and an enteric soluble coating coated on the pellet core. The pellet core mainly comprises tamsulosin or pharmaceutical acceptable salts thereof, and a sustained-release framework material formed by a hydrophilic gel material and an insoluble sustained-release material. The pellet is prepared by a manner of extrusion-spheronization. The tamsulosin enteric coated sustained-release pellet is prepared simply and has stable release rate, capability of complete release and good repeatability.
EP1768670A1 Use of flibanserin for the treatment of anorexia nervosa The invention relates to a method for the treatment of anorexia nervosa comprising the administration of a therapeutically effective amount of flibanserin.
EP1019087B1 Ganglioside immunostimulating complexes and uses thereof The present invention relates generally to an immunostimulating complex comprising one or more gangliosides and more particularly to an immunostimulating complex comprising at least one of the gangliosides GM2, GD2, GD3 or GT3. The present invention is useful, inter alia, as a prophylactic and/or therapeutic agent in the treatment of tumours, and more particularly, melanomas.
CN101537012A Complex vitamin freeze-dried powder injection and preparation method thereof The invention discloses a complex vitamin freeze-dried powder injection prepared from a lipid soluble vitamin, a water-soluble vitamin, a solubilizer and a plasticizer. The invention further discloses a preparation method of the complex vitamin freeze-dried powder injection. The method comprises the following steps: stirring the lipid soluble vitamin, the solubilizer and water for injection for dissolution, and then adding the water-soluble vitamin and the plasticizer, additionally adding the water for injection and keeping stirring for dissolution, and then adding activated carbon for adsorption, adjusting pH value, filtering, bottling, freeze drying, packing and sealing to obtain the finished freeze-dried powder injection. The complex vitamin freeze-dried powder injection employs few subsidiary materials, has simple preparation process, screens and optimizes the freeze-dried process in particular; has low production cost, safe and reliable quality, and is convenient to storage and transportation.
CN103027924A Application of trichoderma pseudokoningii exopolysaccharide as medicine for treating gastric cancer The invention relates to an application of trichoderma pseudokoningii exopolysaccharide as a medicine for treating a gastric cancer, and belongs to the technical field of a medicine and health food. Trichoderma pseudokoningii exopolysaccharide with an antitumor activity provided by the invention can obviously inhibit the growth of human gastric cancer cells BGC-823, MKN-45 and MGC-803 through in vitro administration; explosion of an reactive oxygen in the BGC-823 cell and decreasing of a mitochondrial membrane potential are caused, so that nucleic acid in a tumor cell is cracked, a DNA (deoxyribonucleic acid) segment is produced, a BGC-823 cell cycle is stopped at an S stage, and finally, apoptosis of cancer cells occurs, and therefore, the antitumor effect is produced. The medicine administrated in vivo can inhibit tumor growth of a BGC-823 tumor-bearing mouse, an MKN-45 tumor-bearing mouse and an MGC-803 tumor-bearing mouse, and relieves tumor weight, so that trichoderma pseudokoningii exopolysaccharide has a remarkable antitumor effect.
EP1657244A1 2-thiaquinolizidines as glycosidase and glycosyltransferase inhibitors A process for producing 2-thiaquiolizidines which are glycosidase and glycosyltransferase inhibitors is described. The compounds are of the formula: where x is 0 to 3.
WO2014074952A1 Methods and compositions for localized delivery of agents to hiv-infected cells and tissues The invention provides compositions and methods for delivering an agent to virally infected tissues and/or cells of a subject by conjugating agent-loaded nanoparticles to virus-specific T cells, such as cytotoxic T lymphocytes. The agent may be a latency-reversing drug (LRD), an antiviral agent and/or an agent that enhances cytotoxic efficacy of T lymphocytes.
CN103059084A Acetyl isovaleryl tylosin amide, preparation method and application The invention belongs to the field of medicinal chemistry and discloses an acetyl isovaleryl tylosin amine derivative with anti-mycoplasma and antimicrobial activity, a synthesis method and an application thereof. The preparation method of the compound disclosed by the invention is simple, mild in condition, and high in yield. An external activity test proves that the acetyl isovaleryl tylosin amide provided by the invention has an obvious inbibitional effect on animal mycoplasma and G+, G- infection, and can be applied to the preparation of anti-mycoplasma and antimicrobial drugs.
WO2011065402A1 Indole compound and pharmaceutical use thereof Disclosed are: a therapeutic or prophylactic agent for inflammatory diseases, allergic diseases and autoimmune diseases; an agent for suppressing rejection in organ transplantation; and the like. Specifically disclosed is a compound represented by general formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof. (In the formula, the symbols are as defined in the description.)
CN102178666A Application of Honokiol to preparing drugs for preventing or treating intracranial space occupying lesion and intracranial tissues and organs inflammation The invention relates to the technical field of medicines and aims at solving the technical problem about providing a new effective choice for preventing or treating intracranial space occupying lesion and intracranial tissues and organs inflammation. The scheme for solving the technical problem provides an application of Honokiol to preparing drugs for preventing or treating intracranial space occupying lesion and intracranial tissues and organs inflammation. The invention further provides the application of Honokiol combined with carmustine (BCNU) to preventing or treating primary or metastatic tumors of brain, and the application prospect is bright.
CN1657040A Curcumin and phosphatide composite and its preparation method A curcumin-phosphotide composition is prepared from curcumin or its derivative and phosphotide through proportional compounding. Its advantage is high utilization rate of curcumin. Its preparing process is also disclosed.
US20080069872 Maintenance of therapeutic concentration in blood; core with protective coating The present invention relates to a type of controlled-release multilayered methylphenidate pellet that does not need to be combined with another type of pellet. It allows the maintenance of therapeutic levels in the plasma during 12 hours with a single daily dose, avoiding repeated administrations throughout the day. The controlled-release multi-layered pellet is comprised of an inert core, a first layer that contains methylphenidate and an acid buffering system, a protective layer, a layer of ethylcellulose, that performs the function of controlling the extended release of most of the methylphenidate, and a second layer of methylphenidate, that is responsible for the immediate release of the aforesaid within one hour of administration. The weight ratio between the methylphenidate present in the first active layer and the ethylcellulose is between 1.40:1 and 1.90:1. The multi-layered pellet may possibly have an external coating to protect it from erosion during processing.
EP2695612A1 Use of active substance combinations from urea and carnitine and/or one or more acyl-carnitines used in the treatment and prophylaxis of neurodermatitis and of diabetic foot Use of active compound combinations of urea and carnitine and/or one or more acyl-carnitines for preventing and/or treating atopic dermatitis and diabetic foot, is claimed. ACTIVITY : Dermatological. MECHANISM OF ACTION : None given.
CN103182045A Medicine for treating tinea of feet and hands and preparation method thereof The invention discloses a medicine for treating tinea of feet and hands. The medicine is prepared from the following ingredients by weight: 10-20 parts of radix stemonae, 5.0-10.0 parts of radix sophorae flavescentis, 5.0-10.0 parts of common cnidium fruit, 3.0-6.0 parts of cortex pseudolaricis, 2.5-4.5 parts of hydnocarpus anthelmintica, 2.5-4.5 parts of broom cypress fruit, 3.0-5.0 parts of cortex phellodendri, 3.0-5.0 parts of dried alum, 0.2-0.6 parts of blister beetle, 0.5-1.0 camphor, 0.5-1.0 parts of menthol, 1-2 parts of salicylic acid, 1-2 parts of benzoic acid, 0.2-0.6 parts of phenol, and 31.6-58.8 parts of ethanol. The medicine has the effects of clearing away heat and drying dampness, nourishing the blood to expel wind, killing parasites to relieve itching, and resisting against germs and relieving pains. The invention further discloses a preparation method of the medicine, which comprises the following steps: drying, crushing and mixing radix stemonae, radix sophorae flavescentis, common cnidium fruit, cortex pseudolaricis, hydnocarpus anthelmintica, broom cypress fruit, cortex phellodendri, dried alum and blister beetle, placing the mixed powder into a supersonic extractor, adding 70% ethanol to extract effective components, preparing the alcohol extract of the effective components, preparing the concentrated extract of the effective components, grinding camphor, menthol, salicylic acid, benzoic acid and phenol in weight part together, dissolving with ethanol to form a co-dissolving solution, mixing the concentrated extract of the effective components with the co-dissolving solution, and forming a mixed solution.
CN101606938A Compound medicine for treating skin desquamation of sweaty hands The invention relates to a compound medicine for treating the skin desquamation disease of sweaty hands, which belongs to a medical preparation, in particular relates to a medicine of vitamin C and vitamin B1 compound for treating the skin desquamation disease of the sweaty hands. The compound medicine comprises the components of vitamin C and vitamin B1, the vitamin C contained in each granule of the medicine is 0.1mg to 15mg, and the vitamin B1 contained in each granule of the medicine is 0.1mg to 300mg. In the method, the vitamin C contained in each granule of the medicine is preferably 10mg, and the vitamin B1 contained in each granule of the medicine is 4mg to 70mg. Furthermore, in the method, the vitamin C contained in each granule of the medicine is preferably 10mg, and the vitamin B1 contained in each granule of the medicine is 60mg. The each time dose of the compound medicine when being taken orally is 0.1mg to 15mg of vitamin C and 0.1mg to 300mg of vitamin B1, and a user takes the compound medicine for three times per day and continuously takes the compound medicine for 7 to 15 days. The invention has low price, no toxic or side effect and oral administration and takes the sum of effect taking and efficiency as the total effective example number, and the total effective rate of the invention is 92.59%.
US20120289555 Novel S-Nitrosoglutathione Reductase Inhibitors The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
WO2010101537A1 Pharmaceutical composition of alendronate and a calcium salt combined in a single dosage form The present invention relates to a pharmaceutical composition comprising a combination of alendronate and a calcium salt in a single dosage form so as to increase patients' compliance and as a result the success of the treatment.
US6908927 Reduction physical cigarette smoking The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to process for preparing them, and to the method of use thereof in the treatment or prevention of disorders associated with a dysfunction of the nicotine receptors.
EP1911760A1 Xanthine oxidase inhibitor A compound represented by the following formula (I) is used as a xanthine oxidase inhibitor: in which R1 is phenyl or pyridyl each optionally having, as a substituent, C1-8 alkyl, C1-8 haloalkyl, C1-8 alkoxy, carboxyl, halogeno, hydroxyl, nitro, cyano, amino, etc.; R2 is cyano, nitro, etc.; X is oxygen, sulfur, etc.; and Y is sulfur, NH, etc.
US7056655 Methods for monitoring and guiding therapeutic suppression of parathyroid hormone in renal patients having secondary hyperparathyroidism The present invention relates to novel methods for monitoring and guiding therapeutic suppression of parathyroid hormone in renal patients having secondary hyperparathyroidism. One determines and monitors the level of parathyroid hormone agonist and parathyroid hormone antagonist in the renal patient. The parathyroid hormone suppressing therapeutic is administered to the patient so as to minimize the level of parathyroid hormone antagonist.
US20120165390 Compositions and Methods for Therapy and Diagnosis of Cancer The present invention is directed to siRNA molecules which specifically target and cause RNAi-induced degradation of mRNA from TPTE genes, so that the protein product of the TPTE gene is not produced or is produced in reduced amounts. The siRNA compounds and compositions of the invention are useful for treating diseases which require inhibition of TPTE expression for their treatment, in particular cancer pathologies. The present invention also includes methods which make possible to assess and/or prognose the metastatic behaviour of a cancer disease and/or the occurrence of a relapse of cancer.
WO2010034996A1 Crystalline acid addition salts and their use as enzyme inhibitors A crystalline acid addition salt of the compound of formula (I), said salt being selected from the hydrogen sulfate, p-toluene sulfonate, naphthalene-2-sulfonate, fumarate, and ethanesulfonate salts thereof. The said salts are inhibitors of human neutrophil elastase (HNE), and thus of use in the treatment of inflammatory conditions, including those of the respiratory tract, especially when administered by inhalation for pulmonary delivey.
EP1534258A2 AGONISM OF THE 5HT 2a RECEPTOR FOR TREATMENT OF THERMOREGULATORY DYSFUNCTION The present invention relates to a method for treating thermoregulatory disorders by administering compounds and compositions of compounds which by modulating 5HT levels activate the 5HT2a receptor. The invention also relates to therapy using 5HT1a antagonists and SRIs in combination and pharmaceutical compositions and products containing it.
WO2009095377A1 Spiro compounds as npy y5 receptor antagonists The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, (I) wherein R is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; Z1 is H, C1-C4 alkyl or F; Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond; A is a 6-10 membered aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or -C(=O)-X; or O(CH2)0-1R1; B is hydrogen or is a 5-6 membered heteroaryl, or a 4-6 membered heterocycle, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom; R1 is -(C1-C4)alkyl(C1-C4)alkoxy; or C3-C8 cycloalkyl; or R1 is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; X is OR2 or NR3R4; R2 is C1-C4 alkyl; R3 is hydrogen or together with R4 and the nitrogen form a 5-6 saturated membered ring; R4 is C3-C8 cycloalkyl; processes for their preparation, intermediates used in
CN102743371A Medicine for treating retinal neovascular diseases The invention relates to a medicine for treating retinal neovascular diseases, which is prepared from nafamostat mesylate; moreover, antibodies of endotoxin molecules C3a and/or C5a of a complement system are selectively added in the medicine. According to the invention, the nafamostat mesylate is used for preparing the medicine for treating retinal neovascular diseases, wherein the nafamostat mesylate acts on complement way; in addition, antibodies of C3a and C5a polypeptides are added to the medicine to generate neutralization; therefore, the growth of retinal neovascular can be controlled more effectively. The prepared medicine can be a novel medicine for treating retinal neovascular diseases, thereby providing a new thought for clinically treating various retinal neovascular diseases.
WO2013131931A1 Aminomethylene pyrazolones with therapeutic activity A compound having the structure according to formula III wherein: X is NH or S;R1 is H or (1C-4C)alkyl;R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N-, O-or S-atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro;R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, a monocyclic non-aromatic ring having one or more N-, O- or S-atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N-, O- or S- atoms in the ring, whereby each of these optional substituents is optionally further substituted with (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, halogen, nitro or (1C-2C)dioxol forming a ring;or R3 and R4 form together pyrrolyl, imidazolyl, pyrazolyl, pyrrolidinyl, pyrrolinylimidazolidinyl, imidazolinyl, piperidyl, piperazinylmorpholinyl, each optionally substituted with (1C-6C)alkyl, phenyl(1C-4C)alkyl, phenylketo(1C-4C)alkyl; R5 is H, Cl, F, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; R6 is H, (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, nitro or halogen;R7 is H,F, Cl, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; or pharmaceutically acceptable addition salts thereof for use in treatments of carcinoma, in particular to delay, prevent or reverse metastasis in prostate cancer.
CA2666446A1 Compositions for prostate and menstrual/menopausal related health The disclosure provides compositions and methods and maintaining prostate health and relieving menstrual and menopausal related symptoms. The compositions comprise at least two of an icariin component, a quercetin component, a Maca component, a cocoa polyphenols component, and/or a rosmarinic acid component.
US20090269281 Calcium/Calmodulin-Dependent Protein Kinase Kinase as a Control Point for Cardiac Hypertrophy The present invention includes compositions and methods for treating a patient with cardiac hypertrophy by providing the patient with an effective amount of a Calmodulin kinase kinase inhibitor that is sufficient to treat cardiac hypertrophy.
CN1742741A Medicinal composition containing amino glucose and calcium agent and vitamin D and use thereof The present invention discloses a medicine composite containing aminoglucose, calcium agent and vitamin D as effective active components and different auxiliary materials, said medicine composite can be used for preventing and curing osteoporosis and osteoarthropathy, and can be made into various do sage forms of tablet, capsule, soft capsule and microcapsule, etc.
WO2009123221A1 Pyrimidine derivative having cell-protecting activity and use thereof Disclosed is a prophylactic or therapeutic agent for nerve diseases such as ischemic brain diseases and neurodegenerative diseases or the like or a prophylactic or therapeutic agent for diseases for which an antioxidant activity is effective, which can act as a cell-protecting agent, particularly an inhibitor of cerebral cell injury or cerebral cell death. Specifically disclosed is a compound represented by formula (1), or a pharmaceutically acceptable salt, solvate, hydrate or prodrug thereof.
CN103304546A Pyrazoline derivatives comprising 1,4-benzodioxan structure, and preparation method and application thereof The invention relates to pyrazoline derivatives comprising a 1,4-benzodioxan structure. The derivatives are characterized in that the derivatives have a general formula as the following. R1, R3, and R3 in the formula are as the following. The pyrazoline derivatives can be adopted as potential antibacterial and antitumor medicines. The invention discloses a preparation method of the derivatives.
CN102860983A Novel pharmaceutical composition of 2-(4- isobutylphenyl) propionic acid The invention discloses a pharmaceutical composition. The mol ratio of arginine and ibuprofen is more than 1:1. The pharmaceutical composition is characterized in that the composition exists in an aseptic powder form or in a solution form that the arginine is subjected to acid protonation or is combined with acid to form salt. The invention also discloses a method for preparing the composition. The composition can be used in injection administration in a freeze-dry or non-freeze-dry form and in oral administration, excellent effects of the ibuprofen, such as antipyresis, anti-inflammation and analgesia, are kept, and the incidence rate of common adverse reaction of gastrointestinal tracts and cardiovascular systems of the ibuprofen is reduced to certain extent. Besides, the preparation of the composition is stable, and phenomena that total impurities and foreign matters fail to meet standards during sterilization, degerming and long-term placing are reduced.
US20070117853 (+)-3-acetyl-6-chloro-2-[2-(3-(N-(2-hydroxyethyl)-N-isopropylamino)propoxy)-5-methoxyphenyl]benzothiazoline; kappa -opioid receptor agonist The invention aims to provide a drug having an activity on inhibiting a decrease in pain threshold. Since a κ-opioid receptor agonist effectively inhibits the decrease in pain threshold, it is useful as an inhibitor of pain threshold decrease.
WO2014138907A1 Substituted aromatic compounds for the treatment of pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis The present invention relates to substituted aromatic compounds for use in prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis, where the compound has the following formula: or a pharmaceutically acceptable salt thereof, wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)-(CH2)n-CH3 or CH(OH)-(CH2)n-CH3 wherein n is 3 or 4; R1 is H, OH or F; R2 is H, OH, F or CH2-OH; R3 is H, OH, F or CH2Ph; R4 is H, OH or F; Q is 1 ) (CH2)mC(O)OH wherein m is 1 or 2, 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)-C(O)OH, 5) CF2-C(O)OH, or 6) C(O)-C(O)OH.
CN101822644B Micro-balloon injection for pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate The invention discloses a micro-balloon injection for a pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate, which is characterized by comprising cefmenoxime hydrochloride, anhydrous sodium carbonate, polylactic acid- polyethylene glycol block copolymer, poloxamer 188, glycerol and mannitol. The optimal scheme of the invention is the micro-balloon injection for the pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate, which is characterized by comprising 1 part of cefmenoxime hydrochloride, 0.12-0.18 part of anhydrous sodium carbonate, 1.2-4.5 parts of polylactic acid- polyethylene glycol block copolymer, 0.8-2 part(s) of poloxamer 188, 0.5-1 part of glycerol and 3-6 parts of mannitol. Compared with the prior art, the micro-balloon injection for the pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate prepared by the invention has high stability, the preparation process is simple and is suitable for industrial production, and has high encapsulation efficiency. As anhydrous sodium carbonate is used as a latent solvent, the re-dissolution is good, and has an appropriate slow-release effect.
US20080044472 Photoresponsive Hydrogels Disclosed are photoresponsive hydrogels. The compositions disclosed herein can be prepared by polymerizing a hydrogel precursor and a spiropyran. The properties of the disclosed compositions can be changed by exposure to light, pH, and temperature. Methods of using the disclosed compositions to deliver pharmaceutical actives are also disclosed.
WO2014121155A1 Methods of treating iron deficiency with soluble ferric pyrophosphate The invention provides for methods of treating iron deficiency and methods of reducing or eliminating the dose of erythropoiesis stimulating agent for increasing or maintaining hemoglobin levels in the target range in a subject suffering from anemia comprising administering soluble ferric pyrophosphate in an amount effective to maintain or increase Hgb levels in the subject.
US20060128634 Alpha, alpha-disubstituted benzylglycine derivatives as HIV protease inhibitors This invention relates generally to alpha,alpha-disubstituted benzylglycine derivatives of the formula: or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits including the same, methods for using the same for treating viral infection or an assay standards or reagents, and intermediates and processes for making the same.
WO2014046441A1 Dolastatin-10 derivative, method of producing same and anticancer drug composition containing same The present invention provides a dolastatin-10 derivative having excellent anticancer activity, a method of producing the same and anticancer drug composition containing the same as an active principle.
US20060057156 Materials and methods for inductions of immune tolerance The invention provides methods of inducing immune tolerance to target antigens in individuals seropositive for certain infectious agents by administration of epitopes derived from those infectious agents. Epitopes derived from viruses which carry homologues of interleukin 10 (IL-10) in their genome, such as Epstein Barr Virus and cytomegalovirus, are particularly suitable for these purposes. Particularly preferred is the use of the EBV LMP1 protein and epitopes thereof.
WO2010097816A1 Flavanoid compounds and process for preparation thereof The present invention relates to flavanoid compounds of general formula (X1) wherein: R1 is selected from a group consisting of morpholinyl, N-methyl piperizinyl, piperidinyl and N,N'-dimethylamino groups, and n ranges from 3 to 6, and process for preparation thereof. The present invention relates to the demonstration of anti Helicobacter pylori activity and gastric antisecretory activity of semisynthetically designed flavonoid compounds, to be used for the prevention and treatment of gastroduodenal disorders in general and peptic ulcer diseases in particular. The present invention also relates to a hetero-dimeric bi-functional molecule that can be used as monotherapy substituting/replacing/overcoming currently used triple/quadruple therapy, thereby implicating/ anticipating/envisaging its commercial applicability.
EP2334680A2 Hcv protease inhibitors Novel compounds that are potent inhibitors of hepatitis C virus protease are provided. Pharmaceutical compositions containing one or more of these inhibitors, methods of preparing the inhibitors and methods of using the inhibitors to treat hepatitis C and related disorders also are provided.
CN1883590A Method for preparing ganoderma spore oil The invention relates to a process for preparing glossy ganoderma spore oil by using lucid ganoderma spore powder and glossy ganoderma as the raw material, which comprises enzyme method wall-breaking, wet method palletizing, supercritical CO2 extracting, finally carrying out centrifugation.
US20050020665 For example, N-hydroxy-N-(1-benzo[b]thien-2-ylethyl) acetamide,1-(1-Benzo[b]thien-2-ylethyl)-1-hydroxy urea,N-hydroxy-N-(1-benzo[b]thien-2-ylethyl)-N'-methyl urea Use of a compound of the general formula I and/or a pharmaceutically acceptable salt thereof as active ingredient for the preparation of a pharmaceutical composition for the treatment of multiple sclerosis in humans: wherein X represents NCH3, O or S. A represents an unsubstituted C1-4 alkylene or a substituted C1-4 alkylene that is mono- or poly-substituted with substituents independently selected from CH3, CH2CH3, CH2CH2CH3 und CH(CH3)2, M represents H; benzoyl; unsubstituted C1-12 alkanoyl; substituted C1-12 alkanoyl that is mono- or poly-substituted with substituents independently selected from CH3, CH2CH3, F and Cl; unsubstituted C1-12 alkyl; or substituted C1-12 alkyl that is mono- or poly-substituted with substituents independently selected from CH3, CH2CH3, F and Cl; R represents CH3, CH2CH3 or NR1R2, wherein R1 and R2 independently represent H, CH3 or CH2CH3, and Y1, Y2 and Y3 are independently selected from H, CH3, CH2CH3, F and Cl.
CN102580015A Medicament for treating stomach ache and preparation method thereof The invention relates to a medicament for treating stomach ache and a preparation method thereof. The preparation method comprises the following steps of: soaking Chinese angelica, common fennel, star anise, nutgrass galingale rhizome, dahurian angelica root and liquoric root into water, putting into a boiler, decocting and filtering; concentrating into thick paste; grinding clove, frankincense, myrrh and the like into powder, adding into the thick paste, and drying; and grinding into fine powder and performing split charging. The medicament has the advantages of convenience for taking, small dosage, good curative effect and particularly remarkable effect on deficiency-cold stomach ache.
US20090117183 Oral contraceptive containing a gestagen and an estrogen combined with pharmaceutically acceptable auxiliary agents and/or excipients, but not containing lactose, and method of making same The method produces a lactose-free oral contraceptive composition containing a combination of a gestagen and an estrogen together with one or more pharmaceutically acceptable auxiliary agents and/or excipients. The contraceptive composition is a tablet, powder, or capsule that contains the gestagen and estrogen, filler material such as microcrystalline cellulose and a binder such as hydroxypropylcellulose, but no lactose. Preferably the gestagen is dienogest, chlormadinone acetate, or levonorgestrel and the estrogen is ethinylestradiol, 17β-estradiol, or estradiol valerate. A method is provided for improving the prophylaxis of lactose intolerance in women taking oral contraceptives. The oral contraceptive preparations for a standard 28-day cycle or for long-term use contain at least 21 daily dose units of the gestagen and the estrogen in a low-dosage but without lactose and at most 7 daily dose units containing no active ingredient or a placebo.
US20080200472 urinary incontinence, ulcer, inflammatory bowel disease, addiction, Parkinson's, anxiety, epilepsy, seizures, pruritus, psychosis, cognitive disorder, Huntington's chorea, ALS, retinopathy, migraine, vomiting, dyskinesia, depression; Pyridazinylpiperazine compounds; VR1 Vanilloid Receptor 1 antagonists A compound of formula: wherein X is S or O and A, R1, R2, R3, R4, n, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Pyridazinylpiperazine Compound”), compositions comprising a Pyridazinylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD and IBS in an animal comprising administering to an animal in need thereof an effective amount of a Pyridazinylpiperazine Compound are disclosed herein.
CN102247341A Diterpenes natural product inhibitor for main proteases of coronaviruses, such as SARS (Severe Acute Respiratory Syndrome) and the like as well as screening method thereof The invention provides a method for screening a diterpenes natural product inhibitor from henry rabdosia leaves by taking the in-vitro inhibitory activity screening and crystal structures of main proteases of coronaviruses, such as SARS (Severe Acute Respiratory Syndrome), TGEV (Porcine Transmissible Gastroenteritis Virus), AIBV (Avian Infectious Bronchitis Virus), and the like, as a base. The compound with the following structural general formula can effectively inhibit the activity of the main proteases of the coronaviruses.
CN103655556A Anti-inflammatory application of small molecule compound AG-4 The invention discloses anti-inflammatory application of a small molecule compound AG-4, and application in preparing anti-inflammatory drug. The small molecule compound AG-4 is screened through a candidate drug screening platform combining structural biology, information biology and biological activity determination. The small molecule compound AG-4 can realize specific binding with CD147 protein to inhibit inflammatory cell chemotaxis and secretion of chemotaxis; the invention is also suitable for preparing medicines for treating CD147 protein high expression related diseases (such as rheumatoid arthritis).
CN102302505A Medicinal composition for treating pelvic inflammatory disease and application thereof The invention provides a medicinal composition for treating pelvic inflammatory disease and application thereof. The medicinal composition consists of the following components in parts by weight: 1 to 2 parts of berberine hydrochloride, 1.2 to 2 parts of paeoniflorin, 2 to 4 parts of chlorogenic acid, 5 to 10 parts of dextrin, and 90 to 95 parts of ethanol. The medicinal composition provided by the invention has the effects of clearing away heat and toxic material, eliminating dampness and reducing leukorrhea, and regulating menstruation and relieving pain, and has remarkable curative effect on damp-heat chronic pelvic inflammatory disease.
CN1615867A Naloxone hydrchloride freeze-dried powder preparation for injection The freeze dried naloxone hydrochloride powder for injection consists of naloxone hydrochloride in effective medicine amount and proper amount of medicinal carrier. The naloxone hydrochloride content is 0.08-70.59 wt% or 0.1-12 mg; and the medicinal carrier may be one or several of mannitol, glucol, sodium chloride, beta-cyclodextrin, dextran, fructose, sorbic alcohol, etc., is preferably mannitol and glucol and has the ratio in the preparation of 29.41-99.92 wt%.
US7384976 Nebivolol and its metabolites in combination with nitric oxide donors, compositions and methods of use The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.
CN1631372A Microbial drug material, its preparing method and usage The invention discloses a selenium-containing microbiological preparation for treating cancer, wherein the newly screened bacterial is employed for carrying out fermentation to inorganic selenium, so as to transform into nontoxic biological selenium, then composite fermentation is carried out with granulose extracted from natural edible mushrooms. The prepared granulose has higher synthesis effect and better clinical application result.
CN102552253A Skin external agent for eliminating acnes The invention discloses a skin external agent containing rapamycin for eliminating acnes.
US20100004308 Benzofuran-3-yl(indol-3-yl) Maleimides as Potent GSK3 Inhibitors Compounds of formula: and pharmaceutically acceptable salts, esters and solvates thereof, where variables are defined in the specification, useful generally as inhibitors of protein kinases and particularly useful for inhibition of GSK-3. Pharmaceutically compositions and medicaments containing a compound of the invention are provided. The invention provides methods of treatment of protein kinase-related disease, disorders or conditions. The invention provides methods of treatment of GSK-3-related diseases, disorders or conditions. More specifically, methods of treatment of bipolar disorder, including mania, schizophrenia, stroke, epilepsy, motor neuron disease, cranial or spinal trauma, neurodegenerative disorders, including multiple sclerosis (MS), Alzheimer's disease, Fragile X syndrome, autism, Huntington's disease, Parkinson's disease, amylotrophic lateral sclerosis (ALS), AIDS-associated dementia, diabetes, particularly type II diabetes, cardiomycete hypertrophy, reperfusion/ischemia, cancer, particularly colorectal cancer, pancreatic cancer, allergies and/or asthma and hair loss or baldness.
US20080206336 Once-a-day modified release tablet formulation rosiglitazone and metformin; enteric coating to control the rate of release; erosion of coating under pre-determined pH conditions; diabetes mellitus, metabolic syndrome, impaired glucose tolerance or impaired fasting glucose An oral dosage form comprising an erodable core, which core comprises Compound A or a pharmaceutically acceptable salt or solvate thereof and another antidiabetic agent, the core having a coating with one or more openings, characterised in that the coating is erodable under predetermined pH conditions; a process for preparing such a dosage form and the use of such a dosage form in medicine.
CN102872027A Preparation method for medicine granules for treating asthma and pneumonopathy and preparation method for suction type compound aerosol of granules The invention discloses a preparation method for medicine granules for treating asthma and pneumonopathy and a preparation method for suction type compound aerosol of the granules, and relates to the preparation of the medicine granules and suction compound aerosol thereof, wherein the medicine granules comprise one of salts capable of being accepted physiologically, like L-sulfuric acid albuterol, albuterol or albuterol, and budesonide. The medicine components of the suction type aerosol comprise the two active materials, as well as granules formed by one or more than one of cyclodextrin, polysaccharide, a polylactic acid and an antioxidant in a supercritical fluid state, and the average diameter of the medicine granules is 0.2-3 microns. The medicine granules can be prepared to the suction type compound aerosol.
CN101390846A Amoxicillin capsule and production method thereof The invention relates to an amoxicillin capsule and the preparation method thereof, in particular to a method of adopting the micropowder technology to prepare amoxicillin capsules. The method utilizes the micropowder technology to overcome the bad dissolution of the amoxicillin capsule in the prior art; meanwhile, the amoxicillin capsule prepared by the method has the advantages of improving the preparation stability, simplifying the preparation process, reducing the toxic and side effects.
WO2012085003A1 2-hydroxyisoquinoline-1,3(2h,4h)-diones and related compounds useful as hiv replication inhibitors The present invention relates to compounds and compositions acting as inhibitors of HIV integrase. The compound of the invention is of Formula (I), or a tautomer (I') thereof, or a pharmaceutically acceptable salt, or solvate of said compound or tautomer thereof, wherein R1, R2, R3, R4, R5 and R6 have defined meanings.
WO2012118068A1 Antineoplastic agent and manufacturing method and use therefor The present invention relates to substance 3787-5-1 represented by formula (I) and pharmaceutically permissible salts thereof. Substance 3787-5-1 is useful for the prevention and treatment of a disease caused by a cell proliferative disorder, particularly a malignant tumor, because it has antineoplastic activity acting alone and also enhances the antineoplastic activity of other antineoplastic agents. This substance can be produced by culturing a microorganism of the genus Phytohabitans that is capable of producing substance 3787-5-1, particularly Phytohabitans sp. 3787-5, and collecting substance 3787-5-1 from the culture product thereof.
US20120225012 Composition for hard tissue repair The composition for hard tissue repair of the present invention is characterized by comprising 5 to 98.95 parts by weight of a monomer (A), 1 to 75 parts by weight of a (meth)acrylate polymer (B) and 0.05 to 20 parts by weight of a polymerization initiator composition (C) containing an organoboron compound (c1), with the proviso that the total amount of the components (A), (B) and (C) is 100 parts by weight. The composition undergoes small-scale heat generation during curing and can ensure a sufficient working time.
US7138542 Administering a therapeutically effective amount of an alpha2delta ligand other than gabapentin or tiagabine, or pharmaceutically acceptable salt thereof The invention relates to a method of treating tinnitus by administering an alpha2delta ligand such as, for example, a compound of Formula and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or straight or branched lower alkyl, and n is an integer of from 4 to 6.
CN101361730A Use of propofol succinic acid monoester sodium salt in preparing anti-tumor medicine The invention relates to an application of a propofol derivate, namely propofol succinic acid monoester sodium salt (I) in preparing anti-tumor drugs, in particular, the application thereof in preparing drugs for resisting breast cancer, liver cancer or neuroblastoma.
WO2013170637A1 Application of paeoniflorin compound in preparation of antitumor drug An application of a paeoniflorin compound, or a pharmaceutically acceptable salt, solvate, polymorph, enantiomer, or racemic mixture thereof in preparation of drugs for preventing and/or treating tumors. Preferably, the paeoniflorin compound is selected from albiflorin and/or paeoniflorin. The tumors are solid tumors.
US20100311711 Inhibitors of NAAA and Methods Thereof Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.
WO2008027584A3 5- (2-furyl)-1, 3-thiazole derivatives useful as inhibitors of phosphatidylinositol 3-kinase The present invention relates to compounds of formula (I) useful as inhibitors of P13K particularly of P13Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
CN101537188B Pinocembrin and cyclodextrin or cyclodextrin derivative inclusion compound The invention discloses a pinocembrin and cyclodextrin or cyclodextrin derivative inclusion compound, wherein cyclodextrin or a cyclodextrin derivative is used to include the pinocembrin. The inclusion compound contains the pinocembrin and the cyclodextrin or cyclodextrin derivative in a molar ratio of 1:1-100. The inclusion compound can improve the water solubility of the pinocembrin and give good play of the therapeutic action of the pinocembrin. The inclusion compound is suitable for the preparation of sold dosage forms and liquid dosage forms required by clinics, including infusion solution, water injection, powder injection, oral solution, syrup, tablets, capsules, granules and dispersible tablets. The inclusion compound can be used for preparing drugs for preventing and\or treating cardiovascular and cerebrovascular diseases, particularly brain stroke, as well as drugs for preventing and\or treating bacterial and\or fungal infections.
WO2006053487A1 The use of vegetable anthraquinone derivatives and vegetable polysaccharides for treating human immunodeficiency virus (hiv) The use of vegetable anthraquinone derivatives and vegetable polysaccharides for treating human immunodeficiency virus(HIV);the anthraquinone derivatives and polysaccharides were obtained by CO2 supercritical extraction from plants, then the vegetable anthraquinone derivatives and vegetable polysaccharides alone or the mixture thereof were subject to test for inhibiting HIV virus, HIV virus was added to the culture plate containing emodins and Rheum hotaoense polysaccharides good growth of cells and reduction of viral amount were observed. So said emodins and Rheum hotaoense polysaccharides can be used as active ingredient to preparing drugs or foods for treating AIDS.
CN101429107A Lignanoid compounds, producing method, identification method and uses thereof The invention relates to a novel lignanoid compound shown in a general formula (I), wherein 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13. 14, 15, 16, 17 and 18 represent C1, C2, C3, C4, C5, C6, C7, C5, C8, C9, C10, C11, C12, C13, C14, C15, C16, C17 and C18 respectively. The invention also relates to a method for preparing the novel lignanoid compound separated from fructus schizandrae and an identification method. Simultaneously, the invention also relates to application of the novel lignanoid compound in preparing a drug with anti-HIV activity.
US20060074080 Combination product comprising melagatran and an anti-arrhythmic oxabispidenes There is provided a combination product comprising: (1) melagatran or a pharmaceutically-acceptable derivative thereof; and (1) a compound as defined in claim 1 of WO 01/28992 or (2) a compound of Claim 34 of WO 01/28992 or (3) Compound A or B or C or D (or pharmaceutically-acceptable salts thereof) for use in treating arrhythmia or a coagulation controlled complication thereof.
CN103566257A External ointment for clearing heat, drying dampness and removing toxicity The invention discloses an external ointment for clearing heat, drying dampness and removing toxicity. The external ointment is characterized by comprising the following components by weight: 10-20g of gleditsia sinensis, 10-20g of rheum officinale, 10-20g of cicada slough, 10-20g of chaulmoogratree seed, 10-20g of dictamnus dasycarpus turcz, 10-20g of stemona, and 10-20g of pepper. The external ointment plays effects of purging intense heat and removing toxicity, dispelling wind and arresting itching, and killing fungus when being used for treating tinea of feet and hands and tinea corporis, so that the state of illnesses can be effectively treated and healed.
US20080031953 Composition And Method For Treating Or Preventing Psychiatric Symptom The present invention provides a composition comprising precious metal particles for treating or preventing a psychiatric symptom. The composition of the invention is able to improve various psychiatric symptoms and useful for treating or preventing psychiatric disorders.
EP2138180A1 A composition for treating cancer containing a porous silicon nanobomb as an active ingredient Provided is a composition containing a porous silicon nanobomb as an active ingredient for treating cancer. The porous silicon nanobomb can be exploded by NIR light irradiation at a low intensity to selectively destroy cancer cells. Also, porous silicon itself shows good biocompatibility and biodegradability. Thus, the composition of the present invention can be used as an efficient anticancer agent without the accumulation of toxic side effects.
US7109229 Methods and compounds for treating proliferative diseases The compounds disclosed herein are indolocarbazoles of Formula (I), which are potent CDK4 inhibitors, and are useful in the treatment of cell proliferative disorders, including cancer. Formula (I).
CA2746423C Aminopyrazole compounds as chki inhibitors The present invention provides an aminopyrazole compound (see above formula), or a pharmaceutically acceptable salt thereof or a solvate of the salt, that inhibits Chk1 and is useful in the treatment of cancer.
US20100004296 Waterborne topical compositions for the delivery of azelaic acid A waterborne topical composition is designed specifically to address the treatment of acne vulgaris, rosacea, seborrheic dermatitis and other skin conditions. The composition contains effective amounts of essential components azelaic acid, niacinamide, and glycerin to create a rapidly penetrating and non-irritating compound.
CN102491869A Rheumlikiangense extract with liver injury protection activity and preparation method thereof The invention relates to a rheumlikiangense extract with liver injury protection activity, which contains not less than 40 percent of a diphenylethene compound of a structural formula shown below based on the total mass, wherein the diphenylethene compound is extracted from rheumlikiangense; and the vinylidene of the mother nucleus of the diphenylethene compound has a trans-form, and R1, R2, R3 and R4 may be -H, -OH, -CH3, -OCH3, -C6H11O6, -O-C6H11O6 independently. According to the invention, the clear structure, definite composition and mature analysis and detection methods of the active ingredient of the rheumlikiangense extract facilitate the quality monitoring and control of products at different stages, and the rheumlikiangense extract is in accordance with the development trend and requirements of natural medicinal composite preparations. Meanwhile, the invention also discloses the preparation method of the extract.
EP1565451B1 Halothienoyl-cyclopropane-1-carboxylic acid derivatives Compounds of formula (I) wherein R is hydroxy, linear or branched C1-C6 alkoxy, phenoxy, benzyloxy, a group -N(R1R2) wherein R1 is hydrogen, linear or branched C1-C4 alkyl, benzyl, phenyl and R2 is hydrogen or linear or branched C1-C4 alkyl, or R is a glycoside residue or a primary alkoxy residue from ascorbic acid, optionally having one or more hydroxy groups alkylated or acylated by linear or branched C1-C4 alkyl or acyl groups; X is a halogen atom and n 1 or 2 are long lasting inhibitors of kynurenine 3-monooxygenase (KMO) and potent glutamate (GLU) release inhibitors.
WO2009088854A1 Epoxy-guaiane derivatives and treatment of cancer Disclosed are englerins and derivatives (I) thereof useful in the treatment of a number of cancers, particularly renal cancer, as well as pharmaceutical compositions and method of treating a patient with the use of these derivatives. The englerins, for example Englerin A and Englerin B, can be isolated from the plant Phyllanthus engleri or produced by synthetic methods. An example of the englerin derivative is 2'-chloroenglerin A, which has the structure (II), wherein double bond 'a' is E, Z, or a mixture of E and Z.
CN1771931B Use of diterpene compound in preparing medicines with synergistic effect to chemical therapy medicines The present invention relates to the pharmaceutical use of diterpene compound with the general expression as shown or its precursor medicine, and is especially the use of the diterpene compound or its precursor medicine in preparing medicine with synergistic effect on tumor chemotherapy medicine.
US20100285125 Delivery system for poorly soluble drugs The present invention relates to an oral drug delivery system for poorly soluble drugs, which can provide sustained near zero order release of poorly water soluble drugs from erodible matrix systems. Erodible matrix core is prepared using at least one active and erosion modulators in a matrix of low molecular weight and high molecular weight hydrophilic polymers in combination with a pH sensitive polymer which enable uniform hydration, controlled erosion and pH independent drug release through out GIT. The core optionally contains solubilizers. The core is optionally coated using combination of low molecular weight water soluble and water insoluble polymers, plasticizer and fillers, which provides for drug release, following a lag time, which also helps to reduce food effects in the stomach.
US6998407 For prophylaxis and therapy of chronic or acute inflammatory or autoimmune diseases, those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.
US20100068263 Method and Compositions for Stimulation of an Immune Response to TRP2 using a Xenogeneic TRP2 Antigen Tolerance of the immune system for endogenous TRP2 can be overcome and an immune response stimulated by administration of xenogeneic or xenoexpressed TRP2 antigen. For example, mouse TRP2, or antigenically-effective portions thereof, can be used to stimulate an immune response to the corresponding differentiation antigen in a human subject. Administration of xenogeneic antigens in accordance with the invention results in an effective immunity against TRP2 expressed by the cancer in the treated individual, thus providing a therapeutic approach to the treatment of cancers expressing TRP2, such as melanoma.
WO2013000275A1 C-glycoside derivatives Disclosed are compounds as shown as general formula (I), derivatives and uses thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c and X have the definition as same as the description.
WO2009036322A1 Use of propofol prodrugs for treating neuropathic pain Methods of treating neuropathic pain in a patient comprising orally administering a therapeutically effective amount of a propofol prodrug having high oral bioavailability are disclosed.
CN103479784A Medicine for treating rhinitis The invention provides a medicine for treating rhinitis, relating to medicines for treating rhinitis. The medicine is prepared from the following selected raw materials by weight: 100-120g of rehmannia root, 100-120g of Chinese angelica, 8-12g of angelica dahurica, 8-12g of borneol, 8-12g of beewax and 700-800g of sesame oil; the medicine is prepared by the following steps of putting the sesame oil into a pot, heating until smoke appears, cutting rehmannia root, Chinese angelica and angelica dahurica into pieces or strips, putting into the sesame oil, frying until the pieces or strips are slightly brown, fishing the pieces or strips out and then adding borneol and beewax to prepare paste. The medicine has the beneficial effects that the medicine is used externally, takes effect quickly, is safe and reliable and has good curative effects; 61 clinical tests show that the effective rate is 98.4%.
US20080305176 Process For Loading Polymer Particles With Drug The present invention relates to processes for loading microsphere polymer particles with crystallisable drug, in the presence of a crystallisation inhibitor whereby crystallisation of the drug is inhibited. The invention is of particular value for loading polymer beads with paclitaxel, ibuprofen and/or dexamethasone. The polymer is suitably an anionic polyvinyl alcohol polymer.
CN1895265A Active medicinal matter for improving adrenal cortex hormone function prepared by coarse solomon's seal polysaccharide An application of the crude polygonapolyose as the active component in preparing the medicines for promoting the recovery of adrenal cortex function is disclosed.
WO2006134486A2 Alpha-(aryl-or heteroaryl-methyl)-beta piperidino propanamide compounds as orl1-receptor antagonists This invention provides the compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 and R4 independently represents hydrogen or the like; R5 represents aryl or the like; -X-Y- represents -CH2O- or the like; and n represents 0, 1 or 2.These compounds have ORL1 -receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
WO2012166151A1 Use of dihydropyridophthalazinone inhibitors of poly (adp-ribose) polymerase (parp) in the treatment of myelodysplastic syndrome (mds) and acute myeloid leukaemia (aml) Disclosed herein are compounds of Formula (I) where R1, R2, R3, R4, R5, A, B, Y, and Z are as defined herein for use in the treatment of MDS or AML. Also disclosed are the methods of identifying a patient with MDS or AML who is sensitive to treatment with a PARP inhibitor, in particular a compound of Formula (I).
CN103110729A Pull-aright paste for facial paralysis, and preparation method and use method thereof The invention relates to pull-aright paste for facial paralysis, and a preparation method and a use method thereof. The pull-aright paste is prepared by the raw material medicines in parts by weight as follows: 12-18 parts of radix angelicae, 10-15 parts of radices sileris, 12-18 parts of sophora japonica branch, 10-15 parts of ramulus mori, 10-30 parts of willow branch, 12-18 parts of castor bean, 300-500 parts of sesame oil, 300-500 parts of rosin powder and 10-18 parts of verdigris. The paste provided by the invention is externally applied to treating facial paralysis, the patients are free from pains, the treatment time is short, and injection, medicines and hospitalization are avoided; the paste is convenient to use and does not affect work and study to a large extent; for ordinary patients, one paste is used once for about 15 days to cure the facial paralysis; for individual patients, the paste is applied twice for 20-30 days to cure the facial paralysis; and according to the paste for treating facial paralysis provided by the invention, the effective rate is 100%, and the cure rate is over 90%.
WO2013084130A1 Multicomponent crystalline system of voriconazole with fumaric acid A novel solid form of Voriconazole comprises the active ingredient (2R,3S)-2-(2,4- difluorophenyl)- 3-(5-fluoropyrimidin- 4-yl)-1 -(1H-1,2,4-triazol-1 -yl)butan-2-ol and fumaric acid. The solid composition comprising the two components shows improved properties such as water solubility, crystallization behavior and stability.
EP2121714A1 Aminoglycoside antibiotics targeting bacterial 16s ribosomal rna The present invention relates to paromamine-based compounds according to formula (I) having selective antimicrobial activity directed at ribosomal 16S RNA. Furthermore, the invention is directed to the use of said compounds for preparing a medicament, pharmaceutical preparations and methods for preparing said compounds.
CN103040095A Osmanthus scent snuff The invention belongs to the technical field of snuff products, relates to osmanthus scent snuff made of pure natural raw materials, and further relates to a preparation method of the snuff. The snuff is made of the following natural raw materials, by weight, 100-500 parts of green tea leaf, 0.05-0.35 part of musk, 50-150 parts of fructus amomi, 10-90 parts of adenophora stricta, 100-300 parts of folium mori, 0.1-0.4 part of borneol, 0.03-0.10 part of asarum, 0.01-0.09 part of rhinoceros horn, 5-15 parts of rhizoma acori graminei, 25-125 parts of tobacco leaf, 2-6 parts of agilawood, 2-6 parts of flos caryophylli, 5-25 parts of radix angelicae, 2-6 parts of menthol and 50-150 parts of red wine. The snuff is smoked by osmanthus and has faint scent of osmanthus. The snuff can energize and restore consciousness, enables a nasal cavity to breath smoothly and can assist users to quit smoking.
CA2526943C Compositions comprising hepoxilin analogs and their use in the treatment of cancer Methods and pharmaceutical compositions are provided for treating a cancer in a mammal by administration of a hepoxilin analog, and for promoting apoptosis in a cancer cell.
US20060029661 Orally administrable pharmaceutical formulation The present invention relates to pharmaceutical formulations for oral administration through a soft gelatin capsule, wherein the pharmaceutical dosage form has pseudoephedrine hydrochloride as the active pharmaceutical ingredient. The active pharmaceutical ingredient, pseudoephedrine hydrochloride as an active is embedded in a suitable matrix, wherein said matrix composition is characterized by reducing the extractability of the pseudoephedrine hydrochloride.
WO2014039223A1 Diagnosis and treatment of aspirin-exacerbated respiratory disease (aerd) Described herein are assays and methods relating to the diagnosis, prognosis, and treatment of aspirin-exacerbated respiratory disease (AERD) by detecting and/or measuring the level of platelet-bound leukocytes in a subject or a sample obtained from a subject.
EP1019066B1 Methods and compositions for preventing and treating heartburn A method for preventing heartburn episodes in a patient at risk to development of heartburn, comprising administering to the patient, following the heartburn inducing event but prior to development of heartburn, a composition comprising a pharmaceutically effective amount of an H2 antagonist and an amount of antacid having between about 15 mEq and 46 mEq acid neutralizing capacity.
EP2329824A1 Novel pharmaceutical composition for treatment of nociceptive pain Provided is a novel potent pharmaceutical composition for treating nociceptive pain. The present invention relates to a pharmaceutical composition for treating nociceptive pain, containing a morpholine derivative or a pharmaceutically acceptable salt thereof, as an active ingredient. The present invention is useful in providing an excellent pharmaceutical composition for treating nociceptive pain. In addition, the present invention is particularly useful in providing a pharmaceutical composition for treating pain accompanying a disease selected from the group consisting of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, spondylosis deformans, gouty arthritis, juvenile arthritis, scapulohumeral periarthritis, and cervical syndrome, lumbago, lumbago accompanying spondylosis deformans, menalgia, pain and tumentia after inflammation, operation or injury, pain after odontectomy, and cancer pain. In addition, the present invention is particularly useful for alleviating pain in a damaged cartilage region, and is particularly useful for osteoarthritis in which NSAIDs are not effective.
US8278298 Prophylaxis, therapy of Alzheimer's disease, Pick's disease; administering phenothiazine compound such as methylene blue A composition and use thereof for the prophylaxis or treatment of Alzheimer's disease, motor neurone disease, Lewy body disease, Pick's disease or progressive supranuclear palsy. The composition includes an agent which modulates or inhibits tau-tau association and which does not inhibit tau-tubulin binding. In the method the agent is administered to an individual in order to achieve the desired therapeutic effect. Preferably the agent which is administered is a phenothiazine compound.
CN101721374A Ecabet sodium granules and preparation method thereof The invention relates to Ecabet sodium granules and a preparation method thereof. The preparation method provided by the invention can obviously improve the taste of the Ecabet sodium granules and enhances the obedience of patients.
US20140080846 Method of treating orphan respiratry diseases using doxofylline A method of treating orphan respiratory disease.
EP1335687B1 Method for restoring a damaged or degenerated intervertebral disc The present invention relates to a minimally-invasive method for restoring a damaged or degenerated intervertebral disc at an early stage. The method comprises the step of administering an injectable in situ setting formulation in the nucleus pulposus of the damaged or degenerated disc of a patient. The formulation once injected combines with nucleus matters and host cells, and becomes viscous or gels in situ within the annulus fibrosus of the disc for increasing the thickness and volume of the damaged or degenerated disc. The formulation is retained within the disc for providing restoration of the damaged or degenerated disc.
CA2371393C Use of bismuth subgallate in inhibition of production of nitric oxide synthase The present invention discloses the new use of bismuth subgallate for the manufacture of a medicament for inhibiting of the production of nitric oxide synthase or treating diseases in a subject in which nitric oxide production is implicated. Also disclosed is the new use of bismuth subgallate in combination with borneol for the manufacture of a medicament for inhibiting the production of nitric oxide synthase or treating diseases in a subject in which nitric oxide production is implicated.
US20100272763 Skin external preparation and method of producing the same A skin external preparation includes an oil-in-water emulsion composition. The emulsion composition contains first oil droplet particles having a minimum particle diameter of 200 nm or more and second oil droplet particles having an average particle diameter of 70 nm or less. The first oil droplet particles contain a first functional oil component, and the second oil droplet particles contain a second functional oil component. A method of producing the skin external preparation includes mixing a first emulsion containing the first oil droplet particles having a minimum particle diameter of 200 nm or more and a second emulsion containing the second oil droplet particles having an average particle diameter of 70 nm or less
CA2334711C Medicaments containing bisphosphonic acids and derivatives thereof which are provided for preventing and treating autoimmune diseases and allergies The invention relates to the use of bisphosphonic acids and the derivatives thereof for producing medicaments for preventing and treating autoimmune diseases or allergies combined with the autoantigens specifically used for treating the respective autoimmune disease or combined with the allergens specifically used for treating the respective allergy.Some examples of the bisphosphonic acids or derivatives thereof which are used according to the invention include amino-hydroxy-methylidene-bisphosphonic acid (AMP), 2-amino-1-hydroxyethylidene-1,1-bisphosphonic acid (AEP), pamidronic acid, alendronic acid, 2-amino-1-hydroxyhexylidene-1,1-bisphosphonic acid (AEP), amidinomethylene-bisphosphonic acid (AEP), ibandronic acid. risedronic acid, zoledronic acid, cimadronic acid, and tiludronic acid. Some examples of autoimmune diseases in which bisphosphonic acids or the derivatives thereof can be used include rheumatoid arthritis, severe myasthenia, diabetes mellitus, uveitis, and scleroderma. The bisphosphonic acids or the derivatives thereof and the autoantigens or allergens can be applied simultaneously or in succession. The preparations of the combinations can be used in solid form, as ointments, as solutions or as sprays.
WO2008138843A1 Imidazopyridines and triazolopyrimidines useful for the treatment of joint degenerative & inflammatory diseases Novel fused pyrazine compounds are disclosed that have a formula represented by the following (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammation, rheumatoid arthritis and others.
CN103505422A Solubilized emodin drug-loaded pellet core, colon-targeted pellet and preparation method thereof The invention relates to a solubilized emodin drug-loaded pellet core, a colon-targeted pellet and a preparation method thereof. The solubilized emodin drug-loaded pellet core is prepared by the following steps: emodin and PVPK29/32 are dissolved in ethanol solution and are sprayed to a blank pellet core through the fluidization prescription method; the weight ratio of the emodin and PVPK29/32 to the blank pellet core is 1: 10-6: 10; in the prescription process, the atomization pressure is 1.0-2.0 Pa, the fluidization pressure is 0.5-1.5 Pa, the material temperature is 36-38 DEG C, and the rotating speed of a constant flow pump is 8-12 rad/min; and the emodin colon-targeted pellet is prepared by covering the drug-loaded pellet core with one or several covers of a time lag time, a pH dependence layer and an enzyme contact layer. The solubility of the indissolvable emodin is greatly improved; the colon located release of the emodin can be achieved inside and outside the body through the targeted pellet; and prominent protection effect on the gut barrier function of rat severe acute pancreatitis model is achieved.
US8119819 Malonyl-CoA decarboxylase inhibitors useful as metabolic modulators The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.
CA2807747A1 Anti-microbial metal organic frameworks The present invention relates to metal organic framework materials which possess anti-microbial properties. The present invention also provides methods of preparing such metal organic framework materials and uses of the metal organic framework materials to prevent or treat microbial infections, or provide surfaces which limit contamination by micro-organisms.
WO2009051796A2 2,5-diaryl selenophene compounds, aza 2,5-diaryl thiophene compounds, and their prodrugs as antiprotozoal agents Novel dicationic 2,5-diaryl selenophene compounds are described. Also described are novel aza analogues of dicationic 2,5-diaryl thiophenes. The presently disclosed dicationic compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, and/or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic compounds display good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.
US20100172835 Methods and compositions for synaphically-targeted treatment for cancer Disclosed are compositions and methods useful for targeting therapeutics to cancerous cells and tumors. The disclosed targeting is useful for delivering therapeutic and detectable agents to cancerous cells and tumors.
WO2007072503A2 Combinations for managing inflammation and associated disorders Pharmaceutical compositions comprising at least one analgesic and anti-inflammatory compound(s) that inhibits both cyclooxygenase (COX) and lipooxygenase (LOX) as active agent in combination with at least one another active agent(s) optionally with other pharmaceutically, acceptable excipients is provided. Also described are process for preparation of such compositions and method of using such compositions for the management of inflammation and pain and/or other associated disorders.
CN103463109A Application of Phyllanthoid A in preparing medicament for preventing and treating hepatic injury The invention discloses Phyllanthoid A capable of protecting D-galactosamine (D-GalN) induced acute hepatic injury of mice and CCl4 induced acute hepatic injury of mice. Therefore, Phyllanthoid A can be used for preparing a medicament for preventing and treating hepatic injury or hepatitis, and is disclosed for the first time. The frame model belongs to a brand-new frame model, and Phyllanthoid A has a strong activity in treating hepatic injury, has a highlighted substantial characteristic, and is remarkably progressed in resisting hepatic injury.
CN1833653A Application and prepn. process of shiyacha total flavone An application of Shiyachaí»s flavone in preparing the medicine and functional health-care food for preventing and treating hyperlipemia and the diseases caused by hyperlipemia of people and mammal and the additive of food or forage for regulating blood fat is disclosed. Its preparing process is also disclosed.
EP1729807B1 Combination therapy with azd-2171 The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with a taxane; to a pharmaceutical composition comprising AZD2171 and a taxane; to a combination product comprising AZD2171 and a taxane for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and a taxane; to the use of AZD2171 and a taxane in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.
WO2004069173A3 Methods for modulating an inflammatory response The inventive subject matter relates to novel methods for modulating an immune response in an animal, which comprises administering to said animal an effective amount of an agent that increases IL-27R/WSX-1 activity. Further, the inventive subject matter relates to pharmaceutical compositions comprising an effective amount of an agent that increases IL--27R/WSX-1 activity.
US7244722 5-HT2A receptor related disorders; such as 1-(2-(2-fluoro-4-nitrophenoxy)ethyl)-3-(1piperazinyl)-2(1H)-pyrazinone Compounds of the general formula (I): wherein m, n, R1, R2, R3 and R4 are as described in the specification. Further included are pharmaceutical compositions comprising the compounds, processes for their preparation, as well as the use of the compounds for the preparation of a medicament for the treatment of 5-HT2A receptor-related disorders or medical conditions.
CN101411695A External-use bactericidal medicine for skin and mucous membrane The invention relates to an external sterilizing medicine for skin and mucous membrane, which has good stability and strong sterilizing capability. The invention adopts the technical proposal that the external sterilizing medicine for the skin and the mucous membrane is characterized by containing bromized biethylene diammonium and benzalkonium bromide. The external sterilizing medicine combines the bromized biethylene diammonium and the benzalkonium bromide, has synergism, can reach synergistic effect, has more stability and stronger sterilizing capability, can inactivate hepatitis B surface antigen, and can effectively kill gram-negative bacteria, gram-positive bacteria, colon bacillus, staphylococcus aureus, candida albicans, and the like.
EP2070513A1 Antioxidant combinations with 6,7 disubstituted 2.2-dialkylchromanes or chromenes Topical cosmetic or pharmaceutical composition (A) contains at least one 6,7-disubstituted-2,2-dialkyl- chroman or -chromene compound (A1) and at least one additional antioxidant (A2). Topical cosmetic or pharmaceutical composition (A) contains at least one 6,7-disubstituted-2,2-dialkyl- chroman or -chromene compound (A1), of formula (I) or (II), and at least one additional antioxidant (A2). (A2) is one or more of: flavonoids; polyphenols; catechols; ubiquinones of formula (III); pentaerythritol-tetrakis[3-(3,5-di-tert -butyl-4-hydroxyphenyl)propionate]; urocanic acid; carotenoids; (iso)ascorbic acid or derivatives; ferulic acid; ethyl ferulate; caffeic acid; rosmarinic acid; 2,6-di-tert-butyl-4-methylphenol; tert-butyl-4-methoxyphenol and/or plant extracts. [Image] R 1> and R 2>hydroxy, methoxy or 2,2,2-trifluoroethoxy; R 3> and R 4>1-4C alkyl; n : 6-10. - ACTIVITY : Dermatological. No details of tests for dermatological activity are given. - MECHANISM OF ACTION : Free radical scavenger.
EP1208338A4 Methods and apparatus for producing phase change ice particulate saline slurries A phase change particulate saline slurry and methods and apparatus are provided for producing phase change particulates saline slurries. In one method for producing phase change particulates saline slurries (300), water and a first set amount of sodium chloride are provided to produce a saline solution (302). The saline solution is cooled to a set temperature (304). A selected percentage of chunk ice is broken into ice particles having a small size (306). Next a second set amount of sodium chloride is added and distributed for smoothing of the ice particles (308). If the slurry is to be used later, the slurry is stored in a highly insulated container while maintaining low level of slurry mixing for maintaining optimum slurry fluidity as indicated in block (310). The total saline solution concentrations resulting from the total of the first set amount and the second set amount of added sodium chloride are preferably in the range of about 0.5 % to 6.0 %. The loadings or percentage of ice particles are preferably in the range of 5 % to 50 % and have a size of about 1 mm or less and a generally smooth shape.
WO2013171687A1 1-(p-tolyl)cyclopropyl substituted bridged spiro[2.4]heptane derivatives as alx receptor agonists The present invention relates to 1 -(p-tolyl)cyclopropyl substituted bridged spiro[2.4]heptane derivatives of formula (I), (I) wherein R1 is as defined in the description, their preparation and their use as pharmaceutically active compounds.
CN102716498A Drug liposome capable of efficient and highly specific killing of P53 gene mutation type of breast cancer cells The invention discloses a drug T-VISA-miR34a liposome capable of efficient and highly specific killing of P53 gene mutation type of breast cancer cells. A T-VISA-miR34a treatment carrier capable of efficient and highly specific killing of P53 gene mutation type of breast cancer cells has a nucleotide sequence shown as a SEQ ID NO.1. The drug T-VISA-miR34a liposome capable of efficient and highly specific killing of P53 gene mutation type of breast cancer cells includes a liposome and a T-VISA-miR34a treatment carrier encapsulated by the liposome; and the T-VISA-miR34a treatment carrier has a nucleotide sequence shown as a SEQ ID NO.1. Encapsulated and delivered by the liposome, the T-VISA-miR34a treatment carriers of the invention enrich in the breast cancer site, and can efficiently target breast cancer BCL-2 and CD44 targets, completely or incompletely pair with 3 ' UTR, degrade mRNA of the target gene or inhibit its translation and lead to apoptosis of breast cancer cells without killing the normal cells. The drug can be delivered systemically, has advantages of high gene expression amount, long time, high efficiency, exact efficacy, low toxicity and side effect, no toxicity on kidney or liver, and has broad prospects in the treatment of P53 mutation type breast cancer.
CN101053592B Medicinal composition for treating impaired glucose tolerance and preparation method thereof The invention relates to a medicine combination for treating the impaired glucose tolerance and the preparing method thereof. The medicine combination is mainly composed of balsam pear, mulberry leaf,sanchi, glossy privet fruit, fiveleaf gynostemma herb, chromium picolinate, and zinc gluconate. It is a preparation produced by pharmacological acceptable carrier or excipient, containing capsule, granule, tablet, soft capsule, dropping pill and etc, which is suitable for the patent with impaired glucose tolerance and forepart diabetes. The research indicates that the invention can reduce the blood sugar, decline the insulin resistance, enhance the insulin sensitivity, protect the beta cell function, reduce the serum total cholesterol and serum triglyceride without side and poisonous effects.
CN1638781A Carbon monoxide as a biomarker and therapeutic agent The present invention relates to the user of carbon monoxide (CO) as a biomarker and therapeutic agent of heart, lung, liver, spleen, brain, skin and kidney diseases and other conditions and disease states including, for example, asthma, emphysema, bronchitis, adult respiratory distress syndrome, sepsis, cystic fibrosis, pneumonia, interstitial lung diseases, idiopathic pulmonary diseases, other lung diseases including primary pulmonary hypertension, secondary pulmonary hypertension, cancers, including lung, larynx and throat cancer, arthritis, wound healing, Parkinson's disease, Alzheimer's disease, peripheral vascular disease and pulmonary vascular thrombotic diseases such as pulmonary embolism. CO may be used to provide anti-inflammatory relief in patients suffering from oxidative stress and other conditions especially including sepsis and septic shock. In addition, carbon monoxide may be used as a biomarker or therapeutic agent for reducing respiratory distress in lung transplant patients and to reduce or inhibit oxidative stress and inflammation in transplant patients.
CN1823832A Medicine and fool dual purpose vitamin microelement nutritive product for preventing ane treating cataract and its manufacturing method A nutritive product used as both medicine and food for preventing and treating cataract is prepared from vitamins and trace elements. Its preparing process is also disclosed.
WO2008011363A2 Quercetin-containing compositions This invention relates to a composition containing quercetin, vitamin B3, and vitamin C. Also disclosed is a method of using the composition for enhancing physical or mental performance or treating various diseases or disorders.
CN101829070A Clarithromycin slow-release dispersible tablets and preparation method thereof The invention discloses clarithromycin slow-release dispersible tablets and a preparation method thereof. The clarithromycin slow-release dispersible tablets contain clarithromycin serving as an active ingredient of medicaments and are prepared by the following steps: adopting various pharmaceutical engineering methods; covering protective coatings; and adding fillers, disintegrating agents, flavoring agents, lubricating agents, and the like serving as auxiliary materials; and preparing by a specified preparation method. The dispersible tablets have the characteristics of good friability, rapid disintegration, good mouthfeel, convenient administration, carrying and storage, and the like, and particularly can be taken without water and maintain stable blood concentration for a long time in vivo. Therefore, the patient compliance is improved, and the curative effect of the medicaments is improved.
EP2279735A2 Compositions comprising crystalline trans-(+/-)-delta-9-tetrahydrocannabinol Pharmaceutical compositions comprising the cannabinoid active pharmaceutical ingredient, crystalline trans-(±)-Δ9-tetrahydrocannabinol, and formulations thereof are disclosed. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of crystalline trans-(±)-Δ9-tetrahydrocannabinol. In specific embodiments, the crystalline trans-(±)-Δ9-tetrahydrocannabinol administered according to the methods for treating or preventing a condition such as pain can have a purity of at least about 98% based on the total weight of cannabinoids.
US6908930 4-substituted 7-AZA-indolin-2-ones and their use as protein kinase inhibitors This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of Formula 1 and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, X, Y, and Z are defined herein. The invention further relates to pharmaceutical compositions and dosage forms comprising compounds of Formula 1 and to methods of their use for the treatment and/or prevention of diseases such as, but not limited to, cancer.
EP2651409A1 Novel pharmaceutical formulation comprising nsaid and cyclodextrin The present invention provides a liquid composition in comprising an aqueous solution of an NSAID and one or more cyclodextrins.
EP1830884A1 Treatment of inflammatory diseases An aqueous solution of at least one polyether polyol in a fluid for administration to a mammal, such as a human being, wherein the at least one polyether polyol has a molecular weight of from 200 to 4000 and is dissolved in the aqueous fluid in a concentration of from 0.01 to 10 mg/ml, preferably from 1 to 10 mg/ml.
CA2777352A1 A novel process for the preparation of prostaglandins and intermediates thereof This invention relates to novel process for the preparation of prostaglandin compounds having formula (K), wherein R is selected from the group consisting of C1-C7 alkyl; C7-C17 aralkyl wherein the aryl group is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and (CH2)nOR2 wherein n is from 1 to 3 and R2 represents a C6-C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and R1 is selected from OR3 and NHR3 wherein R3 is C1-C6 alkyl, H; and dashed lines represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.
WO2014111457A1 Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R1, R2, R3, R4, R5, L, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
CN1985848B Compound vitamin and mineral preparation for prenatal taking The present invention relates to a kind of compound vitamin-mineral preparation for prenatal taking and belongs to the field of health care medicine. The compound vitamin-mineral preparation consists of carotene, vitamin A, vitamin E, folic acid, vitamin B1, vitamin B2, nicotinamide, vitamin B6, vitamin B12, vitamin D3, vitamin H, pantothenic vitamin, Ca, Mg, I, Fe, Cu and other minerals. It has reasonable recipe, good nourishing health function and no side effect, and is especially suitable for pregnant women to take.
US20100266674 L-oddc prodrugs for cancer The main drawback in the use of most nucleoside anticancer agents originates from their hydrophilic nature, of which property requires a high and frequent dosage for an intravenous administration. Unlike other nucleoside anti-tumor agents, troxacitabine appears to predominantly enter tumor cells by passive diffusion rather then by using nucleoside transporters, although this may be model dependent. Accordingly, in the present work, a small library of twenty troxacitabine prodrugs has been synthesized using a parallel approach in order to evaluate the relationship between the lipophilicity of the prodrugs and their antitumor activity. Biological evaluation of the prodrugs on two non-small cell lung cancer cell lines (A549 and SW1573) and in pancreatic cell lines clearly showed better antitumor activity than that of troxacitabine, with IC50 values in the nanomolar range.
US6994863 Pharmaceutical and cosmetic carrier and composition for topical application A pharmaceutical or cosmetic carrier or composition for topical application characterized by rheological properties which render the carrier or composition semi-solid at rest and a liquid upon application of shear forces thereto. The composition or carrier are prepared by mixing 1–25 percent of a solidifying agent and 75–99 percent of a hydrophobic solvent, by weight, wherein at least one of them has therapeutic or cosmetic benefits, in the presence or absence of a biologically active substance.
WO2014036654A1 Compounds and methods for selectively targeting cancer stem cells Described are compounds and methods useful for selectively targeting cancer stem cells. The compounds preferentially induce differentiation and/or reduce the proliferation of cancer stem cells relative to normal stem cells. Compounds useful for selectively targeting cancer stem cells include polyene macrolides such as Nystatin or Amphotericin B, analogs thereof and pharmaceutically acceptable salts thereof.
US7135476 Corticotropin releasing factor antagonists; anxiolytic agents; (2,3,5',6',-Tetrahydro)-2'-methyl-4'-(N-propyl-N-cylopropylmethyl-amino) spiro[(1H)indene-1,8'-(7H)quinazoline]; (2,3,5',6',-Tetrahydro)-2'-methyl-4'-(N-propyl-N-cylopropylmethyl-amino) spiro[(1H)indene-1,7'-(5H)cyclopentapyrimidine] Compounds of the formula (I): and pharmaceutically acceptable salts or prodrugs thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
WO2008023063A3 Treatment of cartilage disorders with fgf-18 This invention concerns the treatment of cartilage disorder and osteoarthritis in particular. More specifically, it relates to the use of FGF-18 in treatment regimens and for the manufacture of a medicament for the treatment of patients having a cartilage disorder such as osteoarthritis, such as for example knee osteoarthritis or secondary hip osteoarthritis. Specifically provided is a preferred treatment scheme comprising once weekly administration of an FGF-18 compound per treatment cycle.
EP1267827B1 Use of an aqueous solution for the treatment of try eye The present invention is directed to a method of treating dry eye by instilling eyedrops of a composition containing a cationic cellulosic polymer. Such compositions have been found to alleviate the symptoms of dry eye without requiring the presence of anionic therapeutic agents. Low ionic strength solutions are particularly preferred.
CN102988609A Anti-inflammatory medicament The invention discloses an anti-inflammatory medicament, which comprises the following raw materials in parts by weight: 3 to 6 parts of scorpion, 0.2 to 0.5 part of sulfur, 0.1 to 0.6 part of toad venom, 4 to 7 parts of Indian stringbush root, 1 to 4 parts of morinda officinalis, 2 to 3 parts of cortex albiziae, 2 to 5 parts of dayflower, 3 to 5 parts of honeysuckle, 2 to 4 parts of affine cudweed, and 1 to 3 parts of avicennia prickly ash root. The anti-inflammatory medicament has the functions of diminishing inflammation and counteracting toxic substances, activating meridians to stop pain, clearing heat and removing toxicity, diminishing swelling to remove stasis, dispelling melancholy and regulating blood, calming mind and eliminating swollen welling-abscess, and can be used for preventing and treating diseases, reinforcing immunity and resisting aging.
WO2006014325A3 C-met modulators and method of use The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides appropriately functionalized 5,6-fused bicyclics which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, and flt-3, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
CN103462955A Application of Nardoaristolones A in preparation of medicaments for treating stomach cancer The invention discloses application of Nardoaristolones A in preparation of medicaments for treating stomach canner, and belongs to the technical field of new application of the medicaments. In vitro MTT (3-4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anti-tumor activity evaluation discovers that Nardoaristolones A also has a remarkable effect on inhibiting the growth of human stomach cancer cell strains HGC-27, MGC-803, BGC-823 and SGC-7901, so that Nardoaristolones A can be used for preparing the medicaments for resisting the stomach caner, and has a good development and application prospect, prominent substantive features and significant progress.
WO2006090848A1 Method for detection of nucleotide polymorphism in gene used for diagnosing effect of methotrexate therapy in rheumatoid arthritis patient A method for determining an effect of methotrexate in a rheumatoid arthritis patient and a method for determining the amount to be administered to the patient before the administration, both characterized by detecting a single nucleotide polymorphism in nucleotide 3435 in exon 26 of ABCB1 gene.
WO2008104187A1 Pharmaceutical composition comprising glibenclamide coenzyme q10 and vitamins for the treatment of diabetes 1- Suffering of some diabetic patients from complication of diabetes. 2- The real Causes of cadiac diseases and other disorders in diabetic patients. 3- Importance of addition of some elements as effective substance to drugs used in diabetes treatment to protect diabetic patients from complications of diabetes. 4- Co-enzymeQ 10 is a giant step in nutritional science protects patient from heart muscale weakness and other diseases due to having diabetes. 5- Diabetes damages some essential elements important for enzymes formation and essential amino acid production and its lack leads to appearance of many psychic and somatic symptoms. 6. The solution is addition of; - Vit.BÌ 75mg - Vit.B12 150mcg - Folic Acid 200 meg -Vit.C 80 mg -Vit.E 200 mg - Co-enzymeQ 10 30mg To drugs used to lower the blood sugare level as a protection and prophylaxis for diabetic patients.
CN1729986A Anti-scar drug film and its preparing method The invention provides a cicatrix-resisting membrane comprising a medicinal membrane, wherein the medicinal membrane is a silicon gel film containing medicament of triamcinolone acetonide acetate and silica oil. The invention also discloses the process for preparing the membrane.
CN103654011A Physiotherapeutic pillow capable of calming nerves and assisting in sleeping The invention relates to the field of health care products, and provides a physiotherapeutic pillow capable of calming nerves and assisting in sleeping. The physiotherapeutic pillow is characterized in that filler is composed of raw materials including codonopsis pilosula, bighead atractylodes rhizomes, rhizoma smilacis glabrae, astragalus membranaceus, angelica sinensis, polygala tenuifolia, fried jujube kernels, elecampane, caulis lonicerae, six-eared blumea, cassia seeds and loadstone, wherein the raw materials are manufactured by processes of weighing, smashing, mixing, bagging, suturing, disinfection, subpackage and the like. The physiotherapeutic pillow has the effects of calming the nerves and assisting in sleeping.
CN1927841A Carbonyl additive derivative of geldanamycin benzoquinone, preparation method and use thereof The present invention relates to geldanamycin type carbonyl radical added benzoquinone derivative and its preparation process as well as the medicine composition with the compound as active component and its use. The compound is prepared through fermentation with, say, pseudostreptoverticillium, and it is proved experimentally that the compound may be used in preparing cell period inhibitor and antitumor preparation.
US7001890 Pharmaceutical compositions comprising a polynucleotide and optionally an antigen especially for vaccination The present invention relates to pharmaceutical compositions comprising at least one fragment of a polynucleotide, preferably at least one antigen, and optionally a pharmaceutically acceptable carrier and/or diluent. In accordance with the present invention was found that the introduction of the pharmaceutical composition into vertebrates will achieve regulation of growth, induction of cellular transcription and translation, protein synthesis, protein expression or protein secretion. The pharmaceutical compositions are useful in vaccination protocols but also in any other therapeutic situation in which immunomodulation is of benefit, such as sub-optimal immune responses, reaction to pathogens, tolerance or autoimmunity.
US20110311533 Regulation of protein level The invention relates to regulating the level of a membrane-anchored target molecule using PrP or a fragment thereof and a polyanion. Direct or indirect methods for targeting protein downregulation, mediated through PrP or a fragment thereof and a polyanionare are described. This represents a method for treating/preventing a disease, disorder or condition comprising administration to a subject in need of a therapeutically amount of a chimeric protein comprising PrP or a fragment thereof and a protein of interest, the DNA encoding the chimeric protein, the vector encoding the DNA or host cell harboring the DNA encoding the chimeric protein and a subsequent polyanion administration. It provides a pharmaceutical composition comprising a carrier and a chimeric protein comprising PrP or a fragment thereof fused to a protein of interest, the DNA encoding the chimeric protein, the vector encoding the DNA or host cell harboring the DNA encoding the chimeric protein.
US20050158291 Pet food composition for skin photoprotection An ingestable composition for the photoprotection of the skin of pets which comprises a photoprotecting effective amount of i) at least one probiotic lactic acid bacterium or a culture supernatant thereof, and ii) at least one yeast and/or a carotenoid or derivative, included into an ingestable carrier.
US7255884 Composition for treatment of asthma A pharmaceutical preparation of Chinese herbal medicines for tonifying the kidneys and alleviating asthma is disclosed herein. The Chinese herbal medicines include Perilla Frutescens, Prunus Armeniaca, Glycyrrhiza Uralensis, Scutellaria Baicalensis, Coptis Chinesis, Tusilago Farfara, Stemona Sessilifolia, Fritillaria Cirrhosa, Pheretima Aspergillum, Psoralaea Corylifolia, Codonopsis Pilosula, Hordeum Vulgara, Massa Fermentata Medicalis, Schisandra Chinesis, and Gypsum. The preparation is used to treat thousands of patients suffering from asthma with an effective rate of 93%. The present preparation can relieve cough, expel phlegm, resist airway allergic inflammation reaction, improve pulmonary function, partial pressure of the oxygen in the blood, increase CD2, CD4, CD4/CD8, reduce IgE in blood, increase CAMP, reduce CGMP, stabilize mast cells, and inhibit the release of histamine, which make it capable of stopping an asthma attack.
CN101537013A Application of nanometer polysaccharide for preparing antineoplastic medicament The invention discloses application of nanometer polysaccharide for preparing an antineoplastic medicament. The medicament is prepared by modifying a high relative molecular mass (varying from 1 thousand to hundreds of thousands) polysaccharide into a low relative molecular mass (less than 1,000 nanometers) polysaccharide antineoplastic preparation, and the microparticle has targeting performance superior to that of an original molecule; and the main chemical components of the polysaccharide comprise glucans of beta-1-3D, beta-1-4D, beta-1-6D, and the like. The application of the nanometer polysaccharide for preparing the antineoplastic medicament mainly relates to the field of immunology, in particular to various biological activities and functions of cancer immune therapy, and the like.
EP1575552A2 Metal-containing materials, compositions and methods Metal-containing materials, compositions and methods are disclosed. The metal-containing material can be, for example, an antimicrobial material, an anti-biofilm material, an antibacterial material, an anti-inflammatory material, an anti-fungal material, an anti-viral material, an anti-cancer material, a pro-apoptosis material, anti-proliferative, MMP modulating material, an atomically disordered, crystalline material, and/or a nanocrystalline material. In certain embodiments, the metal-containing material is an atomically disordered, nanocrystalline silver-containing material.
WO2014150395A1 Anti-pcsk9 compounds and methods for the treatment and/or prevention of cardiovascular diseases Disclosed are compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), and methods of using these modulators to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia.
CN101045066A Temperature sensing matter used for preparing medicine to inhibiting tumor angiogenesis, and its use A temp sensitive material for preparing the medicines to prevent and suppress the tumor angiogenesis and in turn to prevent and treat cancers is prepared from N- isopropylacrylamide and acrylamide or N,N-dimethyl acrylamide through copolymerizing.
WO2013104933A1 3,3-diphenyl-n-(1-phenylethyl) propan-1 -amine : as a new selective ligand of the sigma-1 receptors, with anti-apoptotic (cytoprotective) properties and prototypical anticancer activity 3,3-diphenyl-N-(l-phenylethyl) propan-l-amine (fendiline): as a new selective ligand of the sigma-1 receptors, with anti-apoptotic (cytopro- tective) properties and prototypical anticancer activity. This invention concerns the prototypical profile of selective sigma-1 ligand and the putative therapeutical properties of the compound 3,3-diphenyl-N-(l-phenylethyl) propan-l-amine (DPPA) and its pharmaceutically acceptable salts, with cytoprotective activity, more specifically for neurons against the neurodegenerative diseases (e.g. Alzheimer's disease, Huntington's disease, Parkinson's disease) via their anti-apoptotic properties induced by their selective sigma-1 agonism. Concerning the cancer cells, DPPA e hibited pro-apoptotic properties associated with neuroprotective activity originating a prototypical anticancer profile consisting in synergistical association with the clinically used anticancer drugs with its analgesic and neuroprotective activities antagonizing the neuropathic pain induced by the later.
WO2011080269A3 Pharmaceutical preparations comprising a cos releasing compound The present invention relates to pharmaceutical compositions comprising a COS releasing compound according to formula (I) and to methods of preparing such compositions. Said pharmaceutical compositions may preferably be used for the treatment and/or the prevention of cardiovascular diseases.
CA2302411C Improved method for preventing crystal formation in a scopolamine transdermal device A transdermal delivery device comprising scopolamine base and being substantially free of crystalline hydrates and a method of making same.
WO2012043505A1 Novel piperidine derivative and pharmaceutical containing same A novel compound that has the effect of promoting insulin secretion from pancreatic β cells and is useful as a prophylactic and/or therapeutic agent for disorders stemming from hyperglycemia, such as diabetes. A compound represented by general formula (1), a salt thereof, or a solvate of said compound or salt. In the formula, A or B represents a nitrogen atom and the other represents a nitrogen atom or CR8; X represents an oxygen atom, a sulfur atom, −(CH2)n−N(R11)−, or −(CH2)n−CH(R12) −; Z represents a nitrogen atom if Y represents an oxygen atom or a sulfur atom; Z represents an oxygen atom or a sulfur atom if Y represents a nitrogen atom; and R1 through R7 represent hydrogen atoms or other substituents.
CN1876002A A pharmaceutical composition for treating upper respiratory tract infection The invention discloses a medicament for treating upper respiratory tract infection, which is prepared from two raw materials of baikal skullcap root glycosides and bupleurum root volatile fluid.
WO2007139729A8 Novel sulfonamidomethylphosphonate inhibitors of beta-lactamase This invention provides novel β-lactamase inhibitors of the aryl-and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases. Formula (I) or a pro-drug or pharmaceutically acceptable salt thereof, wherein: W represents: Formula (II).
US20050227249 Polymorphisms in the human MDR-1 gene and their use in diagnostic and therapeutic applications Described are general means and methods of diagnosing and treating the phenotypic spectrum as well as the overlapping clinical characteristics with several forms of inherited abnormal expression and/or function of the Multi Drug Resistance-1 (MDR-1) gene. In particular, polynucleotides of molecular variant MDR-1 genes which, for example, are associated with unsufficient and/or altered uptake of drugs by a target cell, and vectors comprising such polynucleotides are provided. Furthermore, host cells comprising such polynucleotides or vectors and their use for the production of variant MDR-1 proteins are described. In addition, variant MDR-1 proteins and antibodies specifically recognizing such proteins as well as concerns transgenic non-human animals comprising the above-described polynucleotide or vectors are provided. Described are also methods for identifying and obtaining inhibitors for therapy of disorders related to the malfunction of the MDR-1 gene as well as methods of diagnosing the status of such disorders. Pharmaceutical and diagnostic compositions comprising the above-described polynucleotides, vectors, proteins, antibodies and inhibitors by the above-described method are provided. Said compositions are particularly useful for diagnosing and treating various diseases with drugs that are substrates, inhibitors or modulators of the MDR-1 gene product.
US20090053138 Stabilized Aptamers to Platelet Derived Growth Factor and their Use as Oncology Therapeutics Materials and methods are provided for producing and using aptamers as oncology therapeutics capable of binding to PDGF, PDGF isoforms, PDGF receptor, VEGF, and/or VEGF receptor or any combination thereof with affinity and specificity. The compositions of the present invention are particularly useful in solid tumor therapy and can be used alone or in combination with known cytotoxic agents for the treatment of solid tumors. Also disclosed are aptamers having one or more CpG motifs embedded therein or appended thereto.
CN103755686A Piperidyl substituted 5-hydroxytryptophane derivatives with anti-platelet aggregation activity The invention relates to the field of pharmaceutical chemistry, particularly piperidyl substituted 5-hydroxytryptophane derivatives (I) with anti-platelet aggregation activity, and a preparation method and pharmaceutical application thereof, wherein R1, R2 and n are defined in the specification. The pharmacodynamical test proves that the piperidyl substituted 5-hydroxytryptophane derivatives have favorable anti-platelet aggregation activity.
WO2011115173A1 Monomaleate of benzothiazine compound Provided is an agent for the treatment and/or prevention of allergic disorders and inflammatory disorders, having good photostability, thermal stability, non-hygroscopic properties and solubility. A monomaleate of a benzothiazine compound is represented by formula (2) (in the formula, l represents an integer of 1 or 2, m represents an integer of 1 or 2, and n represents an integer of 1 to 4).
CN101401807A Uses of selective JAK3 restrainer VI in antiviral mediated acute lung damnification The invention discloses application of a selective JAK3 inhibitor for resisting severe acute respiratory syndrome mediated by SARS virus. The new application of a selective JAK3 inhibitor VI is provided through disclosing a kernel signal transduction molecular mechanism based on that SARS coronavirus drives inflammatory factor to react, and discovering and identifying JAK3 as the key molecular drug target point. The product has obvious anti-inflammation effect without multiaspect toxic side effects of hormone; because of the characteristics of strong selectivity and definite molecular target point, the JAK3 inhibitor VI does not influence the normal antiviral effect of an immunologic system while the JAK3 inhibitor VI plays the function of inflammation resistance; and the inhibitor obviously reduces the virus mediated damage to the immunologic system through inhibiting the reaction of chemotactic factors, thus the selective JAK3 inhibitor is helpful for host immunocytes to generate neutralizing antibodies in time to play the most direct antiviral effect.
CN101165063A Meliacarpinin derivatives, preparation method and use thereof The present invention discloses margosa carbiline derivative and its preparation process and use. The margosa carbiline derivative is the compound as shown, and its optical isomer, medicinal salt, solvate, or ester capable of being in vivo hydrolyzed. The process of preparing the compound includes extracting in solvent, extracting in solar solvent of different polarity, separating the extract, chromatographic separation and HPLC purifying. These derivatives may be applied in preparing antitumor medicine, especially leukemia treating medicine. The compound as one new margosa carbiline compound has simple preparation process.
WO2008088030A1 Composition for prevention or treatment of disease associated with thrombus or embolus Disclosed is a composition for the prevention or treatment of a disease associated with thrombus or embolus, which comprises a combination of at least one member selected from the group consisting of clopidogrel and a pharmaceutically acceptable salt thereof and at least one member selected from the group consisting of eicosapentaenoic acid and a pharmaceutically salt or ester thereof as active ingredients.
CN103479612A Pharmaceutical application of nafamostat The invention provides application of nafamostat in preparation of a medicament for treating spinal cord injury. The nafamostat is applied to therapeutic intervention of the spinal cord injury, and experiments show that the nafamostat can reduce apoptosis of cells, promote survival of neurons, inhibit formation of glial scars and remarkably improve the BBB score of a treated animal. Compared with a methylprednisolone medicament applied clinically at present, the nafamostat has the advantages of wider administration window, more lasting treatment effect and better long-term effect.
WO2007011066A1 Fibroblast activator, collagen production promoter, collagen contraction promoter, hyaluronic acid production promoter, atp production promoter, melanin formation inhibitor, and agent for external application to the skin A fibroblast activator, collagen production promoter, collagen contraction promoter, hyaluronic acid production promoter, ATP production promoter or melanin formation inhibitor comprising at least one compound selected from the group consisting of conagenin, a conagenin derivative and pharmaceutically acceptable salts of the conagenin or conagenin derivative as an active ingredient; and an agent for external application to the skin, cosmetic, pharmaceutical or food which is a composition (a wrinkle-ameliorating composition, a skin-whitening composition) comprising the activator, promoter or melanin formation inhibitor. Thus, provided is an agent for external application to the skin, cosmetic (cosmetic composition), pharmaceutical or food which is safe and has a high wrinkle-ameliorating effect. Also provided is an agent for external application to the skin, cosmetic (cosmetic composition), pharmaceutical or food which is safe and has a high skin-whitening effect.
WO2011029782A1 Substituted (heteroarylmethyl) thiohydantoins as anticancer drugs The invention refers to the use of androgen receptor antagonists for the treatment and/or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.
CN103463000A Application of Neonectrolide A in preparing medicament for treating renal insufficiency The invention discloses application of Neonectrolide A in preparing a medicament for preventing and/or treating renal insufficiency, belongs to the technical field of novel application of medicaments, and is disclosed for the first time. The frame model belongs to a brand-new frame model, and Neonectrolide A has a strong activity in inhibiting renal insufficiency, has a highlighted substantial characteristic, and is remarkably progressed in preventing and treating renal insufficiency.
WO2012051246A1 Tapentadol hydrobromide and crystalline forms thereof The present invention provides a salt of Tapentadol, Tapentadol liydrobromide, and crystalline forms of Tapentadol hydrobromide.
EP2015741A2 Histone deacetylase inhibitors for the treatment of neurodegeneration The instant invention is directed to methods for treating neurodegenerative diseases comprising administering an effective amount of a selective histone deacetylase 8 inhibitor to a patient in need thereof.
US20080318882 Method of Delivery of Nucleic Acids to Peripheral Neurons The invention provides for methods for delivering a nucleic acid into a peripheral neuron by identifying a target neuron in a dorsal root ganglion and intrathecally delivering a vector comprising the nucleic acid to the dorsal root ganglion neuron. The nucleic acid may encode a neurotrophic factor that may be used to treat a peripheral neuropathy or, in conjunction with a nerve guide conduit, to treat a transected peripheral nerve.
EP2180899A2 Cytoplasmic malate dehydrogenase (mdh1) targeted treatment for neurodegenerative diseases The present invention provides compositions for treating neurodegenerative diseases, including ALS, involving complex formation of cytosolic malate dehydrogenase with certain neurodegenerative disease-causing proteins, comprising an agent capable of reducing an interaction between a malate dehydrogenase protein and a conformationally altered or mutant protein associated with a neurodegenerative disorder, including mutant SOD1 protein. The present invention also provides methods of identifying an agent capable of treating such disorders, including ALS, comprising testing agents for the ability to disrupt or prevent formation of a malate dehydrogenase complex with a conformationally altered or mutant protein associated with a neurodegenerative disorder, including MDH-mutant-SOD1 complex, and methods of treating neurodegenerative disorders.
CN102949378A Production method of nail-dissolving medicine patch used for treating onychomycosis The invention relates to a production method of a nail-dissolving medicine patch used for treating onychomycosis. According to the invention, 1g of a nail-dissolving paste is extruded to a central position of the nail-dissolving patch, and the nail-dissolving patch is stuck onto a nail lesion area. The central part of the nail-dissolving patch should be positioned at a nail lesion central area. The nail-dissolving patch is replaced once or twice one day, until a dissolved recess with a size of 1cm appears on the nail lesion area; 0.5g of a nail bed reparation liquid is dropped onto the dissolved recess on the nail lesion area; and a certain amount of the nail bed reparation liquid is uniformly applied at the dissolved recess, such that the inner side of the recess is in a vacuum state. Therefore, sterilizing can be sufficiently carried out by the nail bed reparation liquid in an internal vacuum state. According to the invention, an advanced technical formula is adopted, such that a defect of palliative of conventional onychomycosis treatments is overcome, and sterilizing is carried out under a vacuum state. With the medicine patch, onychomycosis can be completely cured. The medicine patch has the advantages of convenient application, no operation, no pain, no side effect, and the like. The medicine patch is worth popularization.
CN101375870A Compound creat injection and preparation method The invention discloses a compound common andrographis herb injection for treating yellow-white dysentery of piglets and a prepration method. The compound common andrographis herb injection is composed of 20-100 parts of common andrographis herb liquid extract, 10-50 parts of mequindoc, 30-100 parts of analgin, 1-20 parts of nicotinamide, 5-50 parts of Tween-80, 10-30 parts of talc powder and 50-300 parts of ethanol with 95 percent. The preparation method is as follows: the components are weighted according to the weight; the common andrographis herb liquid extract is arranged in water for injection with 50 percent preparation amount, the Tween-80 and the talc powder are added for boiling under stirring for 30min, and ethanol is added after the still placement and the filtration; 300 parts of the water for injection are taken, the nicotinamide is added, and the mequindoc is further added after the dissolution for stirring and dissolution; the prepared solution (2mol/L of sodium hydroxide solution or hydrochloric acid solution with 20 percent) is merged for regulating pH value to 6.0, the analgin is dissolved, the stirring and the dissolution are carried out, the mixture is maintained for 15-20min, and the water for injection is added till 1000 parts after the clarification of liquid medicine for preparation. The invention adopts the compound preparation and has the advantages of rapid onset of action, low residues, no rebound and the like; furthermore, the survival rate of pigs is improved and the body weights of the pigs are increased.
US20050032817 Kinesin spindle protein (KSP) inhibitors, e.g., 3-benzyl-2-(1-{(4-bromobenzyl)[2-(dimethylamino)ethyl]amino}propyl)furo[2,3-d]pyrimidin-4(3H)-one; antiproliferative and -carcinogenic agents; side effects reduction; cancers of the brain, genitourinary tract, lymphatic system, stomach, larynx and lung The present invention relates to furanopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
US20120065181 Method of providing neuroprotection using substituted porphyrins Described herein are methods of treating ischemic injury comprising administering to a subject in need thereof a therapeutically effective amount of a substituted porphyrin compound. Also disclosed are methods of providing neuroprotection, methods of treating subarachnoid hemorrhage, methods of treating traumatic brain injury and methods of treating spinal cord injury using substituted porphyrins.
US20080085873 Disease treatment methods The invention relates to the use of compounds to ameliorate or treat a condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3β-hydroxy-17β-aminoandrost-5-ene, 3β-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3α-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3β-hydroxy-16β-fluoro-17β-aminoandrost-5-ene, 1α,3β-dihydroxy-4α-fluoroandrost-5-ene-17-one, 1α,3β,17β-trihydroxy-4α-fluoroandrost-5-ene, 1β,3β-dihydroxy-6α-bromoandrost-5-ene, 1α-fluoro-3β,12α-dihydroxyandrost-5-ene-17-one, 1α-fluoro-3β,4α-dihydroxyandrost-5-ene and 4α-fluoro-3β,6α, 17β-trihydroxyandrostane.
US20130053418 Acyclic organonitro compounds for use in treating cancer The present invention provides acyclic, geminal-dinitro organic compounds, methods of synthesizing the compounds, pharmaceutical compositions, therapeutic methods, and medical kits for treating various conditions using such compounds and pharmaceutical compositions. The compounds and compositions are useful in the treatment of cancer.
CN101683328A Sterilizing agent for aquaculture The invention relates to a sterilizing agent for aquaculture, belonging to the field of aquaculture industry, in particular to a sterilizing agent for sterilizing pathogenic bacteria inside a culturepond. The sterilizing agent is a solution containing the following materials in parts by weight: 85-95 parts of marketed drug-grade dimethyl formamide and 5-15 parts of florfenicol. The sterilizing agent can effectively sterilize various bacteria inside the culture pond, achieve the sterilizing and purifying effects on the culture pond during treatment, not only effectively treat diseased aquaticanimals, but also treat aquatic animals which can not be fed, thereby achieving the technical effect of fundamentally preventing the aquatic animals from being diseased due to the bacteria; in addition, the sterilizing agent changes the usage mode of the florfenicol, can not only act on the body surfaces of the aquatic animals, but also act on the bacteria of a water body through external use, thereby sufficiently developing the drug effect and further achieving better double effects of treatment and prevention.
WO2014075308A1 Pharmaceutical composition for treatment of cancers, lyophilized preparation for injection of the pharmaceutical composition, preparation method for same, and applications thereof A pharmaceutical composition for treatment of cancers, a lyophilized preparation for injection of the pharmaceutical composition, a preparation method for same, and applications thereof. The pharmaceutical composition comprises 200-300 parts of ginsenosides, 48-72 parts of astragaloside, 60-90 parts of syringoside, and 4.2-6.3 parts of cantharidin. The preparation method for the pharmaceutical composition is a conventional method. The pharmaceutical composition and the lyophilized preparation for injection of same are applicable in treatment of cancers such as primary liver cancer, lung cancer, colorectal cancer, malignant lymphoma, and gynecological cancers.
CN103386045A Radix stephaniae tetrandrae-semen coicis-fructus forsythiae pills as well as preparation method and quality standard detection method thereof The invention discloses radix stephaniae tetrandrae-semen coicis-fructus forsythiae pills as well as a preparation method and a quality standard detection method thereof. According to the detection method, the quality of the radix stephaniae tetrandrae-semen coicis-fructus forsythiae pills can be controlled and the curative effect of the pills can be stable. The radix stephaniae tetrandrae-semen coicis-fructus forsythiae pills are prepared from the following raw medicinal materials in parts by weight: 200-300 parts of radix stephaniae tetrandrae, 300-400 parts of semen coicis, 300-400 parts of fructus forsythiae pill, 150-200 parts of semen armeniacae amarae, 150-200 parts of rehmannia, 150-200 parts of fried batryticated silkworm, 300-350 parts of honeysuckle stem, 80-120 parts of cassia twig, 40-60 parts of liquorice and 80-120 parts of talcum powder. The radix stephaniae tetrandrae-semen coicis-fructus forsythiae pills are clinically used for treating diseases caused by stagnancy of hot-dampness and have a good effect. The quality standard detection method of the pills comprises the steps: qualitatively identifying the semen armeniacae amarae, the rehmannia and the fried batryticated silkworm in the raw materials by a microscopic method, qualitatively identifying the semen coicis, the fructus forsythiae and the honeysuckle stem in the raw materials by virtue of thin-layer chromatography and measuring the contents of the radix stephaniae tetrandrae and the fructus forsythiae in the raw materials by virtue of HPLC (High Performance Liquid Chromatography).
CN101550161A Andrographolide derivative, salt, preparation method and application thereof The invention discloses a new water-soluble andrographolide derivative, salt and a preparation method thereof and medical application of the derivative comprising the salt and pharmaceutical composition. The invention also discloses an inhibiting action of andrographolide derivative to macrophage secretion NO induced by LPS, antibacterial action and inhibiting action to pinna swelling induced by xylene, can be used for preparing treating drugs for anti-inflammatory, antibacterial, antivirus and anticancer and can be used for preparing drugs for treating infectious shock, septicemia, inflammatory bowel disease, rheumatoid arthritis and juvenile rheumatoid arthritis.
CA2739948A1 Treating hepatitis c virus infection with over-expression of microrna-196 The present invention is directed to methods of treating cells infected with HCV and mammals suffering from HCV infection by transfecting the infected cells with miRNA-196 mimic. miRNA-196 mimic significantly down-regulates Bach1 protein and HCV gene expression, while also up-regulating HMOX1 gene expression. miRNA-196 binds with the 3'-UTR of Bach1 mRNA to reduce the expression of Bach1. As such, miRNA-196 can play an important role in the regulation of HCV replication and HMOX1/Bach1 expression in hepatocytes. The present invention also provides a formulation for the treatment of cells expressing HCV comprising a therapeutically effective amount of miRNA-196 such that Bach1 and HCV gene expression are down- regulated while HMOX1 expression is increased. The formulations are adapted to enable the transfection of miRNA-196 mimic into hepatocytes expressing HCV proteins.
US20120171129 Inhibition and Dispersion of Bacterial Biofilms with Benzimidazole Derivatives Disclosure is provided for benzimidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.
US20120136037 Deuterium-enriched ruboxistaurin The present application describes deuterium-enriched ruboxistaurin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US8748470 Methods for treating ovarian cancer by inhibiting fatty acid binding proteins The present invention concerns methods and compositions for the inhibition or reduction of the primary tumor and metastasis by inhibition of fatty acid binding proteins.
US7820633 cytotoxic T-cell mediated killing of disease cells that express a weakly immunogenic or non-immunogenic cell-associated polypeptide antigen in an animal by administering a cytotoxic T-cell epitope and a T-helper lymphocyte A method is disclosed for inducing cell-mediated immunity against cellular antigens. More specifically, the invention provides for a method for inducing cytotoxic T-lymphocyte immunity against weak antigens, notably self-proteins. The method entails that antigen presenting cells are induced to present at least one CTL epitope of the weak antigen and at the same time presenting at least one foreign T-helper lymphocyte epitope. In a preferred embodiment, the antigen is a cancer specific antigen, e.g. PSM, Her2, or FGF8b. The method can be exercised by using traditional polypeptide vaccination, but also by using live attenuated vaccines or nucleic acid vaccination. The invention furthermore provides immunogenic analogues of PSM, Her2 and FGF8b, as well as nucleic acid molecules encoding these analogues. Also vectors and transformed cells are disclosed. The invention also provides for a method for identification of immunogenic analogues of weak or non-immunogenic antigens.
CN102247574A Prescription for treating headache For overcoming the shortcomings in the prior art, the invention provides a prescription for treating headache which has outstanding effect and can almost prevent recurrence. The formula of one dose of the prescription comprises 12g of radix curcumae, 30g of wild Cynanchum atratum, 12g of radix gentianae, 15g of Ulmus pumila, 12g of angelica, 3g of asarum, 12g of rhizoma ligustici wallichii, 10g of angelica dahurica, 12g of green tangerine orange peel, 12g of chrysanthemum, 1 g of flower bud of lily magnolia, 20g of polygonatum and 15g of ochre. The medicinal materials are decocted with water, each dose of the prescription is decocted three times, and one dose of the prescription is administered orally every day.
CA2641913A1 1-phenethylpiperidine derivatives and their use as opioid receptor ligands This invention relates to novel 1-phenethylpiperidine derivatives of formuia (I) useful as opioid receptor ligands. More specifically, the invention provides compounds useful as µ opioid receptor ligands. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds of the invention.
US20120329793 Substituted Imidazopyridinyl Compounds The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
CA2595252A1 Novel 6-pyridylphenanthridines Compounds of a certain formula I, in which R1, R2, R3, R31, R4, R5, R51 and Har have the meanings indicated in the description, are novel effective PDE4 inhibitors.
CN102659615A Derivatives of oseltamivir, and method and medical application thereof The invention relates to the field of medical chemistry, in particular to derivatives of oseltamivir (I). R1, R2, L and X are explained in the specifications. The invention also discloses a method for preparing the derivatives of oseltamivir and the purpose of the derivatives for treating infectious diseases, particularly the infectious diseases caused by influenza viruses.
US20110135729 Methods for Controlling Heat Generation of Magnetic Nanoparticles and Heat Generating Nanomaterials The present invention relates to a method for controlling heat generation of a magnetic nanomaterial, comprising the steps of: (a) mixing (i) a nanomaterial precursor comprising a metal precursor material and a predetermined amount of a zinc precursor with (ii) a reaction solvent; and (b) preparing a zinc-containing magnetic nanomaterial from the mixture of step (a) comprising a zinc doped metal oxide nanomaterial matrix; and wherein a specific loss power of the zinc-containing magnetic nanomaterial is varied depending an amount of zinc to be doped, whereby the heat generation of the magnetic nanomaterial is controlled. In addition, the present invention relates to a heat-generating nanoparticle and a composition for hyperthermia. The present invention suggests a novel approach to improve a heat generation of a magnetic nanomaterial. According to the present invention, the specific loss power can be controlled by changing a zinc-content to be introduced into nanomaterials and therefore a composition for hyperthermia showing controlled heat generation potential can be successfully provided.
WO2010062829A1 Tryptophan hydroxylase inhibitors for treating osteoporosis Disclosed are uses of tryptophan hydroxylase inhibitors for increasing bone mass and treating diseases and disorders such as osteopororis. Preferred inhibitors are compounds of the formula (I).
WO2014017573A1 Composition for agent for external use Upon attempting to design a pharmaceutical preparation by mixing minoxidil with a general thickening agent during a process for considering a minoxidil-containing composition for an agent for external use in which dripping is inhibited, it was discovered that the pharmaceutical preparation would have sediments or would cloud and that a sufficient viscosity of the pharmaceutical preparation could not be obtained. The minoxidil-containing composition for an agent for external use of the present invention is characterized by containing minoxidil (a), a hydroxypropyl cellulose and hypromellose (b), ethanol (c), and water (d). Said composition is clear and has a good feel upon use, and dripping of the composition is inhibited.
WO2012136147A1 Benzopyrone derivative and use thereof The present invention relates to the field of pharmaceutical chemistry, and in particular, to a benzopyrone derivative and a use thereof. The benzopyrone derivative is compound having a structure of formula (I) or a pharmaceutically acceptable salt thereof. It has been found by experiments that, this type of compounds is useful in prevention or treatment of neuropsychical diseases.
CN102652754A Treatment of sweating A method of treating non-pathological or pathological sweating is provided, which comprises topically applying to skin in need of treatment for sweating an occlusive composition, for example comprising silicone.
CN103384525A Human milk oligosaccharides for modulating inflammation Disclosed are nutritional compositions including human milk oligosaccharides that can be administered to preterm infants, term infants, toddlers, and children for reducing inflammation and the incidence of inflammatory diseases.
CN101380317B Pharmaceutical composition for easing pruritus The invention relates to a pharmaceutical composite which inhibits and/or relieves pruritus caused by dermatosis, mucosa disease or systemic disease or lesion, and is made from derivatives, salt or solvate of phenyl butyric acid and short chain fatty acid with effective dose and a carrier which is acceptable pharmaceutically.
US20080124416 Therapeutic composition from goji (lycium barbarum l.), methods of making and using The present invention relates to herbal-derived compositions comprising extracts of polysaccharides and carotenoids from Goji species for management of ocular disorders, diabetes, bone metabolism, arthritis, muscle loss, cardiovascular disorders, immunological disorders, fatigue, body weight, sexual disorders, aging disorders, dermatological disorders and neurological disorders. Further provided are methods for making the compositions, and methods for treating subjects with various adverse health conditions with therapeutically or health-promotionally effective amounts of the compositions.
WO2013184734A1 Macrocyclic factor viia inhibitors The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.
CN101143853B Biphenyltetrazoles compounds and preparation method thereof The invention discloses biphenyl tetrazole compounds, which does not easily generate drug resistance, the structure is shown in the figure, wherein, R1 is nonsubstituted or substituted benzene cycle, various five-membered heterocycles, such as pyrrole, furan, thiophene, pyrazole, imidazole, etc. or various six-membered heterocycles, such as pyridine, pyran, pyrimidine, etc.; the substitution of R2 can be the monosubstitution of various halogens and electron-attracting radicels or the polysubstitution of the combination of the halogens and the electron-attracting radicels. The compounds can be used to prepare drugs curing various fungus infections and does not easily generate drug resistance.
CN102247342A New application of alkyl isourea compound The invention discloses a new application of an alkyl isourea compound. The new application is the application of the alkyl isourea compound as shown in a formula (I) or pharmaceutically acceptable salts thereof to the preparation of a gastric cancer cell proliferation inhibitor and the application to the preparation of drugs for preventing and/or treating gastric cancers. An in-vitro cancer cell proliferation resistant experimental result indicates that the alkyl isourea compound has a better inhibiting effect on a human gastric cancer cell line BGC-823, wherein the alkyl isourea compound has the inhibition ratio of 42.16 percent (formula I) on cells of the human gastric cancer cell line BGC-823 when the drug concentration of the alkyl isourea compound is 64 micrometers.
CN102895296A Preparation method of drug, melanterite paste, for treating tinea manuum and tinea pedis The invention relates to a preparation method of a drug, melanterite paste, for treating tinea manuum and tinea pedis. The preparation method comprises the steps of drying dried alum and Liriodendron yellow skins; adding borneol, grinding the above materials into powder; pouring fructus gleditsiae abnormalis, galla chinensis and the like into a pot; decocting, filtering and concentrating to a paste; adding dried alum powder; stirring uniformly; and loading the paste in bottles. The melanterite paste is simple in preparation, is convenient for use, and has especially good effects for the treatment of tinea manuum and tinea pedis.
CN102743413A Preparation method of eye drops for alleviating asthenopia The invention discloses a preparation method of eye drops for alleviating asthenopia, belonging to the pharmaceutical field. The eye drops are a product used for alleviating the asthenopia and contain no antiseptic. Raw materials for producing the product comprise Vitamin B6, taurine, aspartate, borneol, dipotassium glycyrrhinate, pearl powder, coral and injection water. In the production process, packing is reformed, wherein a package with the dosage for two days in winter and one day in summer is adopted, the eye drops are abandoned when used up, and no antiseptic is required to be added. The preparation method of the eye drops for alleviating asthenopia provided in the invention is simple in technology, convenient in operation and low in production cost, and assists in producing the eye drops with good quality.
WO2009147121A1 Carboxyl substituted indoles for use as ppar alpha modulators There is provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts or solvates thereof wherein one of R1 and R2 is H and the other is COOH. The compounds are useful as PPAR modulators.
CN101530487A Application of rubus parvifolius saponin series compound in preparing medicines for treating prostatitis disease The invention discloses the application of rubus parvifolius saponin series compound in preparing medicines for treating prostatitis disease. Animal test result shows that the rubus parvifolius saponin series compound can inhibit weight increment of corpus glandulare prostatae, relieve inflammatory cell infiltration and damage, and has good curing effect to prostatitis. The medicine has high efficiency and low toxicity, small side effect, wide source and low development cost.
CN103316013A Aprepitant composition for injection The invention provides an aprepitant composition for injection, and relates to the technical field of medicaments and preparation of the medicaments. The composition comprises main drugs of aprepitant and melatonin, wherein the melatonin comprises a quick release part and a slow-released part cladded by cyclodextrin. By adopting the aprepitant composition for injection provided by the invention, the treatment effect of the aprepitant is improved; the instability, distribution, fast removal and the like caused by oral absorption of MT (melatonin) are avoided; the first-pass effect of the MT is reduced; the dosage of the aprepitant is reduced; the administration design of combining quick release with slow release accords with the physiological secretion characteristics of the MT; the short half-life period of the MT is solved; the product bioavailability is improved; the composition has synergism on treatment of CINV (chemotherapy induced nausea and vomiting) by the aprepitant; not only can the CINV be treated after combining the MT with the aprepitant, but also the treatment effect of the aprepitant on the CINV is improved; the treatment course is shortened; the dosage of the aprepitant is also reduced; the side effect of the aprepitant is reduced; the human immunity can be improved; certain concentration of melatonin is maintained in blood of a human body, so that the stress reaction of the organism can be effectively reduced; treatment of the CINV is facilitated.
EP2316449A1 Stable pharmaceutical composition containing tranexamic acid and ascorbic acid An object of the present invention is to provide a pharmaceutical composition which is stable without causing discoloration or the like even if tranexamic acid and ascorbic acid are uniformly mixed. The pharmaceutical composition comprising tranexamic acid and ascorbic acid and further comprising an organic acid or an antioxidant other than ascorbic acid or tocopherol as a stabilizer, wherein the components contained in the composition are uniformly mixed.
CN103191431A Coenzyme Q10 sodium chloride injection uneasy to crystallize and preparation method thereof The invention provides a coenzyme Q10 sodium chloride injection uneasy to crystallize and a preparation method thereof. The coenzyme Q10 sodium chloride injection mainly comprises the following raw materials: coenzyme Q10, tween 80, polyoxyl (40) stearate, injection water and sodium chloride. The preparation method comprises the following main steps: step A, uniformly mixing the tween 80 and the coenzyme Q10, heating the mixture in water bath to dissolve the mixture to form yellow transparent liquid, and adequately stirring and processing the yellow transparent liquid with ultrasound; step B, adding the injection water which is preheated to 60 to 80 DEG C into the solution obtained in the step A to obtain an aqueous solution, and adequately stirring and processing the aqueous solution with ultrasound; step C, adding the polyoxyl (40) stearate into the aqueous solution obtained in the step B and adequately stirring and processing with ultrasound; and step D, adding the injection water and sodium chloride, and sterilizing the mixture at high temperature and high pressure after canning the mixture. Through the formulation technology and the use of two cosolvents, the coenzyme Q10 solution can be clear for a long time, so that the product can be normally sold nationwide all the year round, and the sales cost can be greatly reduced.
US20090082461 Deuterium-enriched modafinil The present application describes deuterium-enriched modafinil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US7816408 (N-{5-[(4-chlorophenyl)thio]pentyl}-N-[(1R)-1-(1-naphthyl)ethyl]amine); mimics/blocks effect of extracellular calcium in parathyroid cells, juxtaglomerular/proximal tubule kidney cells, parafollicular thyroid cells, bone osteoclasts, keratinocytes or placental trophoblasts; hyperparathyroidism A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.
WO2011029832A1 Novel thiazol and oxazol hepcidine antagonists The present invention relates to novel hepcidine antagonists of the general structural formula, pharmaceutical compositions comprising the same, and the use thereof as medications, particularly for treating iron metabolism disorders, such as in particular iron deficiency diseases and anemias, in particular anemias in conjunction with chronic inflammatory diseases (ACD, anemia of chronic disease, and AI, anemia of inflammation).
US20110130704 Combination of a light ray and a lipase-bioconvertible compound for improving skin and/or hair appearance The present invention relates to a cosmetic method intended in particular to improve the appearance of the skin and/or hair comprising the simultaneous and/or sequential administration: a) of at least one compound bioconvertible by lipase; and b) of at least one light radiation exhibiting at least one predominant wavelength which activates lipase. In particular, the said light radiation according to the invention exhibits (emits) at least one predominant wavelength which activates lipase ranging from 400 to 510 nm, preferably from 430 to 500 nm, and is preferably used at a dose ranging from 0.01 to 200 J/cm2, preferably from 0.1 to 30 J/cm2, more preferably from 1 to 30 J/cm2, indeed even from 5 to 30 J/cm2. The invention also relates to a composition comprising at least one compound bioconvertible by lipase and at least one compound which emits and/or filters, in particular under exposure to light, a light radiation exhibiting at least one predominant wavelength which activates lipase, as well as to a kit comprising at least one composition comprising at least one compound bioconvertible by lipase as well as a device and/or a compound which emits/filters a light radiation exhibiting at least one predominant wavelength which activates lipase.
CN101298482A Dextran The invention relates to a glucose, in particular to an anti-lung cancer glucose. The main chain of the glucose of the invention is constituted of right repeating structural units with the molecular weight of 1.5 million to 2.5 million Dalton. The glucose of the invention is mainly used for preparing anti-lung cancer drugs.
CN1919288A Decoction medicine for treating acute swollen urethritis and its preparing process Disclosed is a medicinal broth for treating urethritis and its preparing process, wherein the medicament is prepared from the following raw materials (by weight portion): coix seed 25-30g, knotgrass, honeysuckle flower, lysimachia christinae each 18-20g, rhubarb horsetails, Chinese pink herb, corydalis tuber each 12-15g, toosendan fruit 9-12g, plantain seeds, talcum, cape jasmine, clematis stem, rush pith, poria cocos wolf each 8-10g, and licorice root 5-7g. The invention realizes easy material availability, simplified preparation, low cost, and quick effect.
WO2006024627A2 N-2 adamantanyl-2-phenoxy-acetamide derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1, 2, 3, or 4; Z represents O, S, NR6, SO or SO2; R1 represent hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy-; R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of -O-CH2- (a), -NR7-CH2- (b), -(CR8R9)m- (c) and -CR10= (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl; R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR13R14 or C1-4alkyl substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR15R16; R6 represents hydrogen; R11 and R12 each independently represent hydrogen, C1-4 alkyl or C1-4 alkylcarbonyl-; R13 and R14 each independently represent hydrogen, C1-4 alkyl or C1-4 alkylcarbonyl-; R15 and R16 each independently represent hydrogen, C1-4 alkyl or C1-4 alkylcarbonyl-; R17 and R18 each independently represent hydrogen, C1-4 alkyl or C1-4 alkylcarbonyl-.
US20100035927 Medicament for prophylactic and/or therapeutic treatment of alzheimer-type dementia A medicament for prophylactic and/or therapeutic treatment of Alzheimer-type dementia, which comprises donepezil hydrochloride and valproic acid or a salt thereof in combination.
EP1615921A2 Pyrido 2,3-d pyrimidin-7-carboxylic acid derivatives, their manufacture and use as pharmaceutical agents The invention describes compounds of the general formula (I), 5 a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. The compounds show activity as protein kinase inhibitors, in particular src family tyrosine kinase inhibitors, and may therefore be usefull for the treatment of diseases mediated by said tyrosine kinases.
WO2012168411A1 Use of carpipramine in the treatment of psychiatric and developmental disorders in children and adolescents The present invention relates to the selection of patients and treating the latter with carpipramine according to criteria relating to the property of carpipramine of preferentially blocking the alpha2C subtype, which can be used to characterize patients capable of benefiting from treatment with carpipramine, and to exclude those having disorders which cannot be improved by carpipramine.
US7806924 Implantable structures for local vascular delivery of cladribine in combination with rapamycin for restenosis Medical devices, and in particular implantable structures, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic drugs, agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the formation of blood clots. Also, the devices may be modified to promote endothelialization.
CN102617521A Gamma-butyrolactone polyketone compounds having antineoplastic activity The invention relates to the technical field of medicines, in particular to novel gamma-butyrolactone polyketone compounds simplexolide A and simplexolide B having antineoplastic activity which are extracted from marine animal sponges and a preparation process and purposes of compounds. External antineoplastic experiments indicate that compounds simplexolide A and simplexolide B have obvious effects on activity inhibition of human colon cancer cells HCT-116 and SW480, so that compounds can be used for preparing antineoplastic medicines. According to the gamma-butyrolactone polyketone compounds having the antineoplastic activity, novel lead compounds are provided for preparing antineoplastic medicines and scientific evidences are provided for developing and using Chinese marine medicinal resources.
US6946454 Thio-oxindole derivatives This invention relates to methods of co-administering compounds of formula 1 which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, with estrogen, an estrogen, or an estrogen receptor agonist for contraception, hormone replacement therapy, or treating progesterone-related carcinomas and adenocarcinomas.
CN103467281A Phenol derivative and application thereof The invention discloses a phenol derivative and application thereof, belonging to the technical field of medicines. The phenol derivative comprises a compound as represented by a structural formula I, II or III and pharmaceutically acceptable salt, ester and amide thereof. In the formula I, II or III as described in the specification, R1 is selected from the group consisting of an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aryl group, an aralkyl group, halogen and an acyl group, R2 and R3 are independently selected from the group consisting of hydrogen, an alkyl group, a cycloalkyl group, an aryl group, an aralkyl group and an acyl group, respectively, and R4, R5, R6 and R7 are independently selected from the group consisting of hydrogen, an alkyl group, a cycloalkyl group, an aryl group and an aralkyl group, respectively. The invention also discloses application of the compound or the pharmaceutically acceptable salt, ester and amide thereof in preparation of drugs used for treating immune diseases, inflammations or autoimmune diseases.
US7863312 Pyrazolidinone derivatives, e.g., 4-[2-(2-(3-hydroxyoctyl)-5-oxopyrazolidin-1-yl)ethyl]benzoic acid; treating preterm labor, dysmenorrhea, asthma, hypertension, infertility, sexual disorders, undesired blood clotting, bone disorders, (pre)eclampsia, or eosinophil disorders The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteoporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin EP2 and/or EP4 receptors.
CN1966514A Novel acyclic nucleoside phosphonate and its medical use This invention provides trifluoroacetate derivatives of (R)-PMPA or (R)-PMPDAP represented by formula I and their non-toxic biological pharmaceutical acceptable salts, wherein R1 is H or NH2, R2 is H or COO-R3, and R3 is C1-C10 alkyl or phenyl substituted C1-C3 alkyl. This invention also provides drug combinations with acyclic nucleoside phosphonates as shown in formula I and their non-toxic pharmaceutical acceptable salts as active ingredients, and their applications in antiviral drugs, especially in anti-HBV and anti-HIV drugs.
CN101412718A Carbapenem derivative containing sulfenyl heterocyclic amine formyl The invention belongs to the technical field of medicine, and in particular relates to a sulfonyl heterocyclic amino formyl containing carbapenems derivative shown in a general formula (I), pharmaceutically acceptable salts, easily hydrolysable esters or isomers thereof, wherein R<1>, R<2>, R<3>, R<4>, R<5> , R<6> and X are defined in the specification. The invention also relates to a method for preparing the compounds, medical compositions containing the compounds, and application of the compounds to the preparation of medicines for treating and/ preventing infectious diseases.
WO2011081415A2 Sirna for inhibiting c-met expression and an anti-cancer composition comprising the same The present invention provides a small interfering ribonucleic acid (siRNA) which is complementarily bonded to a base sequence of c-Met transcript (mRNA transcript) to suppress c-Met expression in a cell as well as optionally to not induce immunological reactions, and applications of the siRNA for cancer prevention and/or treatment. The siRNA, which is bonded complementarily to the mRNA involved in the encryption of the c-Met, suppresses c-Met expression which is overexpressed in nearly all cancer cells in common due to the RNA interference (RNAi) phenomenon and inhibits the proliferation and metastasis of the cancer cells, thereby making the siRNA very useful as an anticancer agent.
WO2006050314A2 Once a day formulation for phosphate binders A method for reducing serum phosphate in a subject in need thereof comprising administering once per day to said subject a phosphate binder, wherein the phosphate binder has a phosphate binding capacity of at least 52 mole.
CN102038853A Externally applied plaster for treating herpes zoster The invention relates to a formula and a production technique of an externally applied plaster for treating herpes zoster. The invention is characterized in that the externally applied plaster is prepared from rhubarb, radix trichosanthis, pearl powder, coptis, phellodendron bark, cotton rose hibiscus leaf, boneset leaf, bulbus fritillariae cirrhosae, paenoia albiflora, licorice root, frankincense, myrrh, bezoar, borneol, realgar, purslane, impatiens balsamina and vaseline. The drugs are combined to produce synergetic effect. When being applied to the affected part once or twice a day, the externally applied plaster can quickly relieve heat, promote the subsidence of swelling, alleviate pain, remove heat from the blood, promote the blood circulation, accumulate heat and remove toxicity, and the affected part can heal after 5-10 days. The invention has the advantages of easily available raw materials, simple technique, less pain and high safety and reliability, and is convenient in operation; and the effective rate is 100%, and the cure rate is 5%. The externally applied plaster has excellent market prospects and high development value, and is worthy of popularization.
CN101869557A Application of nordihydroguaiaretic acid in preparing drug capable of resisting tumour stem cells The invention relates to a new application of compound, in particular to the application of nordihydroguaiaretic acid in preparing drug capable of resisting tumour stem cells. The nordihydroguaiaretic acid inhibits the activity of arachidonic acid-5-lipoxidase to prevent glioma stem cells from breeding and induce the glioma stem cells to differentiate to astrocyte phenotype; the nordihydroguaiaretic acid has better in vivo curative effect on glioma than the classical glioma chemotherapeutics, i.e. carmustine; meanwhile, the nordihydroguaiaretic acid can obviously inhibit tumour stem cells of gastric cancer, liver cancer, lung cancer, colon cancer, breast cancer and the like from breeding.
US20120128762 Sphingomyelin Liposomes for the Treatment of Hyperactive Bladder Disorders The present invention provides pharmaceutical compositions and methods for the instillation of lipid vehicles comprised of liposomes containing sphingomyelin or sphingomyelin metabolites to prevent, manage, ameliorate and/or treat disorders involving neuropathic pain and aberrant muscle contractions, such as what occurs in bladder hyperactivity disorders such as interstitial cystitis (IC) in animals or humans in need thereof. Also provided is a liposome-based delivery of drugs, e.g., antibiotics, pain treatments and anticancer agents, to the bladder, genitourinary tract, gastrointestinal system, pulmonary system and other organs or body systems. In particular, liposome-based delivery of vanilloid compounds, such as resiniferatoxin, capsaicin, or tinyatoxin and toxins, such as botulinum toxin is provided for the treatment of bladder conditions, including pain, inflammation, incontinence and voiding dysfunction.
CN102727461A Method for preparing tilmicosin phosphate effervescent granules The invention discloses a method for preparing tilmicosin phosphate effervescent granules. The method is characterized by comprising the following steps of: respectively crushing tilmicosin phosphate, tartaric acid, anhydrous sodium bicarbonate, sucrose, lactose and polyethylene glycol, sieving with a 80-mesh sieve, fully mixing, granulating in a boiling bed, reshaping granules to finally obtain the tilmicosin phosphate effervescent granules. According to the method, raw tilmicosin phosphate is directly used as a basic material, and the tilmicosin phosphate effervescent granules are produced by adopting a boiling bed preparation method, so that the production procedures are simplified; the whole method is easy to operate and safe and reliable in production, and has the advantages of energy conservation, consumption reduction, high yield of finished products, low production cost, high working efficiency and the like; and the effervescent granules have the characteristics of convenience in administration, safety, accurate dose and the like.
WO2006094705A1 Ophthalmic uses of s1p receptor modulators The present invention pertains to the use of a S1P receptor agonist in the manufacture of a medicament in the treatment of an ocular disorder.
US20100168205 Methods and Compositions for Prevention or Treatment of RSV Infection Using Modified Duplex RNA Molecules Methods and compositions are provided for the prevention or treatment of RSV infection in a human. The methods include administering one or more doses of a composition comprising an siRNA. The dose can be formulated for topical or parenteral administration. Topical administration includes administration as a nasal spray, or by inhalation of respirable particles or droplets. The siRNA preferably comprises a sense strand and antisense strand with modified nucleotides.
US6872709 Using glycyrrhizin The present invention provides a therapeutic agent and therapeutic method for treatment of mastitis in livestock comprising glycyrrhizin and pharmaceutically acceptable salts thereof as effective ingredients.
US20120052141 Novel use of compounds for treating and alleviating cellulite The present invention is directed inter alia to the use of at least one compound selected from the group consisting of (−)-epigallocatechin gallate, resveratrol, eicosapentaenoic acid, docosahexaenoic acid, rose hip extract/concentrate, hydroxytyrosol, lycopene, lutein, β-cryptoxanthin, zeaxanthin and derivatives thereof, for the treatment of cellulite, for the prevention of the development of mild cellulite, for the prevention of the progression of mild cellulite to severe cellulite, for smoothening the micro relief of the skin, for maintaining or increasing the tensile properties of the skin, and/or for reducing the fat mass and the circumference at the hips and thighs, as well as to the corresponding cosmetic and medical methods.
US20110130365 Fluorinated Heteroaryls The present invention provides Formula (1A) XN O R 3 HN R 5 O R 4 R 2 R 1 (1A) 5 compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the glucokinase enzyme, where X, R 1, R 2, R 3, R 4, and R 5 are as described herein.
CN102988986A Male trait inducer and induction method for pelodiscus sinensis in embryonic periods The invention relates to a male trait induction method for pelodiscus sinensis in embryonic periods. The male trait inducer is characterized in that through dissolving an aromatase inhibitor and an adjuvant into alcohol with the purity of 92-98%, the inducer with an aromatase inhibitor concentration of 50-150 mu g/mu l and an adjuvant concentration of 50-150 mu g/mu l is obtained; and the adjuvant is selected from testosterone, methyltestosterone or testosterone propionate. According to the induction method provided by the invention, the male induction rate can be more than 95% just through spraying the inducer two times at the sex determination key time point in embryonic development, and meanwhile, the normal development and low drug residues of pelodiscus sinensis gonads are ensured; and the induction method provided by the invention is easy to operate, low in cost, and remarkable in economic benefit, thereby being a sex control technology which is worthy of popularization in the existing pelodiscus sinensis breeding.
CN101224196A Ambroxol hydrochloride freeze-dried powder injection and preparing method thereof The invention relates to an ambroxol hydrochloride freeze-dried powder injection and a preparation method thereof. The freeze-dried powder injection comprises ambroxol hydrochloride and mannitol. The ambroxol hydrochloride freeze-dried powder injection prepared by a freeze-drying technology has good stability and high dissolution velocity while all other indexes accord with regulation.
WO2011089559A1 A novel polymorphic form of atorvastatin salts The present invention provides an improved process for the preparation of Atorvastatin of formula (I) or its salts, preferably hemicalcium salt with purity greater than 99.5% using novel salts of Atorvastatin such as N,N- dicyclohexylethylenediamine salt of Atorvastatin and novel polymorph of Atorvastatin sodium salt. Formula (I).
US20090181105 Method of antioxidation, antioxidant-functioning water, and usage of the same The objective of the present invention is to provide an antioxidation method and antioxidant-functioning water that can anticipate high benchmarks of safety on the antioxidation subject such as the human body and reduced environmental burden. An antioxidation method and antioxidant-functioning water that can transform or maintain an antioxidation subject, which is in an oxidation state due to a deficiency of electrons or needs to be protected from oxidation, into a reduced state where electrons are filled by promoting the breaking reaction of molecular hydrogen used as a substrate included in the hydrogen-dissolved water into a product of active hydrogen through a process employing a catalyst, which is a precious metal colloid or a hydrogen oxidation/reduction enzyme (except for those already existing in a living organism), on the hydrogen-dissolved water.
US20110092586 Apoptosis inductor extracted from potato, potato foodstuff containing the inductor, and processed product thereof An apoptosis inductor is formed of an anthocyanin-containing extract obtained from a potato containing anthocyanine in the skin and flesh thereof. The potato is a potato of cultivated species, such as Solanum tuberosum ssp. andigena L. and S. phureja Juz. et Buk., or of hybrid species based on the cultivated species.
US20080275057 Cell cycle G2-checkpoint-abrogating 1-[(2-pyridyl)amino]-azoline-2,5-dione derivatives with at least one halogen group, to selectively sensitize cancer cells to DNA damaging reagents without additional anticarcinogenic treatment; cytolytic agents, antiproliferatives, apoptosis Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.
US7462366 Drug delivery particle A drug delivery particle including a reservoir region having primarily large pores and a metering region. The particle can be highly spherical.
CN102316900A Aniline derivative having anti-rna viral activity Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.
EP1735002A2 Cancer therapy comprising a nuclear receptor ligand and a hdac inhibitor The present invention relates to a novel cancer therapy, particularly, but not exclusively, to a prostate, bladder and breast cancer therapy and to Compositions and medicaments for use in said therapy. In one aspect there is provided a method of treating a patient afflicted with cancer comprising administering to the patient a therapeutically effective amount of a nuclear receptor ligand and an HDAC (histone deacetylases) inhibitor wherein said nuclear receptor ligand is not a ligand for the vitamin D receptor.
US20050281764 Use of EGF-R protein tyrosine kinase inhibitors for preventing photoaging in human skin Photoaging of human skin, such as evidenced by the increased presence of matrix metalloproteinases after exposure to UV radiation, is prevented by pre-treating the skin with an inhibitor of epidermal growth factor receptor (EGF-R) prior to exposure. Such inhibitor are preferably natural, an example of which is genistein. Compositions used for such purposes preferably include an EGF-R as well as another MMP inhibitor, such as a retinoid.
US20090311308 Skincare compositions comprising salicyclic acid There is disclosed a skincare composition suitable for topical application to the skin. The composition comprises salicylic acid or a salt thereof and hydrolysed milk protein. The composition is useful in the treatment of acne.
WO2009056885A1 Use of 3, 11b-cis-dihydrotetrabenazine in the treatment of multiple sclerosis and autoimmune myelitis The invention provides a compound for use in treating multiple sclerosis wherein the compound is a 3, 11b-cis-dihydrotetrabenazine of the formula (Ia): or a pharmaceutically acceptable salt thereof.
CN101219109A Oxolamine sirup and method for producing the same The invention provides an oxolamine syrup and a preparation method thereof, relating to a syrup and in particular to an oxolamine syrup applied to relieve cough and a preparation method thereof. The oxolamine syrup has the advantages of simple preparation method, comparatively good treatment effect and no tolerance and addiction after long-term administration thus especially being suitable for children. Calculated by 1000ml, the syrup contains 6 to 10g of oxolamine, 0.1 to 0.2g of citrate, 0.1 to 0.5g of methylparaben, 0.2 to 2g of gardenia yellow, 1 to 3ml of orange essence, 400 to 600g of sucrose and the rest is water. The water is boiled and the sucrose is added into the water to be stirred and dissolved; the mixture is heated to 100 DEG C, filtered, added with water to reduce the temperature to room temperature and shaken up to obtain syrupus simplex. Oxolamine aqueous solution and the syrupus simplex are mixed, and then the citrate, the methylparaben, the gardenia yellow and the orange essence are added and the mixture is uniformly stirred to obtain the target product.
CN103288880A Semi-sandwich type dual-core organic metal ruthenium compound with anti-tumor activity The invention discloses a semi-sandwich type dual-core organic metal ruthenium compound with anti-tumor activity. The chemical name of the semi-sandwich type dual-core organic metal ruthenium compound is dichloride p-terephthalaldehyde-bis-N4-methyl-thiosemicarbazide-dichloride-dimethyl isopropyl benzene ruthenium (II). A preparation method of the semi-sandwich type dual-core organic metal ruthenium compound comprises the following steps of: 1) preparing a product A; 2) dissolving p-terephthalaldehyde-bis-N4-methyl-thiosemicarbazide; 3) dissolving the p-terephthalaldehyde-bis-N4-methyl-thiosemicarbazide (19mg, 0.1mmol) and the product A (32mg, 0.05mmol) into 6ml of acetone, heating to 45 DEG C, stirring for six hours, to form red transparent solution, standing for 12 hours to generate a great deal of particulate red crystals, namely products. The dichloride p-terephthalaldehyde-bis-N4-methyl-thiosemicarbazide-dichloride-dimethyl isopropyl benzene ruthenium (II) has obvious inhibition effect on gastric cancer SGC7901 tumor cell strains shown by in-vitro tumor cell inhibition activity.
CN101723958A Cefodizime sodium medicament and preparation method thereof The invention provides cefodizime sodium which is prepared by the following steps of: a. firstly, dissolving sodium iso-octoate into an ethanol solution to obtain an ethanol solution of sodium iso-octoate; b. sequentially mixing ethanol, cefodizime acid and triethylamine at 0-30 DEG C and stirring till the cefodizime acid is dissolved; c. decoloring the cefodizime acid solution obtained in the step b and mixing the cefodizime acid solution with the ethanol solution of the sodium iso-octoate obtained in the step a and stirring to obtain an ethanol solution of cefodizime sodium crystals; d. carrying out suction filtering, washing a filter cake with absolute ethyl alcohol and acetone, and carrying out suction filtering to obtain a cefodizime sodium wet material; and e. drying the cefodizime sodium wet material till the weight content of water is within 3.5 percent. The invention also provides a cefodizime sodium medicament and a medicament composition. The obtained cefodizime sodium has good crystal shape and is easy for molding the medicament composition; meanwhile, the cefodizime sodium obtained by the method has high yield, and the solvent use is more environmental-friendly.
CN203315382U Senile plaque removal plaster easy and convenient to use The utility model discloses a senile plaque removal plaster easy and convenient to use. The senile plaque removal plaster is characterized by comprising a medical proof fabric (1), an EVA foaming layer (2), salicylic acid phenol ointment (3) and SOD honey (5). The EVA foaming layer (2) is arranged on the medical proof fabric (1). The salicylic acid phenol ointment (3) is arranged in the middle of the EVA foaming layer (2). The SOD honey (5) is arranged on the salicylic acid phenol ointment (3). The senile plaque removal plaster easy and convenient to use has the advantages that the EVA foaming layer is fixed through the medical proof fabric, treatment medicine is located at the treatment point of the senile plaque, the EVA foaming layer is adopted, and therefore hole shearing, medicine placement and medicine sealing can be conveniently carried out according to the size of the senile plaque; the salicylic acid phenol ointment is adopted to treat the keratosis of the senile plaque, namely the melanocyte, the penetrating capacity is high, and the irritant is low; the SOD honey is adopted to relieve the irritant of the salicylic acid phenol ointment, harmful substances generated in the metabolism are removed, the dermatomyositis is prevented and treated, skin aging resistance is achieved, and the senile plaque is effectively removed.
CN101273974A Sustained-release dropping pill of azithromycin and method of preparing the same The invention discloses an antibiotic drug, aiming at complementing the shortcomings of the existing azithromycin practical preparation, increasing more choices of the drugs for the patients and providing an azithromycin sustained-release drop pill with high bioavailability, rapid onset, high drug content, few administration times, long-acting function, convenient administration, low cost and no pollution in the production. The azithromycin sustained-release drop pill related by the invention takes azithromycin as raw material, and a mixed matrix of a medicinal hydrophilic matrix and a hydrophobic matrix as a carrier for preparation.
EP1538160A1 Substituted Isoquinolin-3-carboxyamides, their preparation and medical use N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy-iso quinoline-3-carboxamide derivatives (I) are new. - N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy- isoquinoline-3-carboxamide derivatives of formula (I) and their salts are new. - A = COOH or CH2OH; - R1 = H or Cl; - R2 = H, 1-8C alkyl, 1-8C alkoxy, Cl, CF3, OH, benzyloxy (optionally substituted by 1-5C alkyl or 1-5C alkoxy) or fluoroalkoxy of formula -O(CH2)x-Q; - x = 0 or 1; - Q = 1-5C alkyl, substituted by 1-11 F; - R3 = F, CN or as for R2; and - R4, R5 = H, 1-5C alkyl, F, Cl, Br, CF3, CN, 1-5C alkoxy or -O(CH2)x-Q. - Independent claims are included for the preparation of (I). - ACTIVITY - Antiinflammatory; Hepatotropic; Nephrotropic; Dermatological; Vulnerary; Antiarteriosclerotic. - In a carbon tetrachloride-induced liver fibrosis model in the rat, N-((1-chloro-4-hydroxy-isoquinolin-3-yl)-carbonyl)-glycine (Ia) at a dose of 2 x 20 mg/kg i.p. per day for 2 weeks inhibited the production of hydroxyproline (as a indicator of collagen production) in the liver by 67%. (Ia) caused no steatosis of the liver when administered to rats at 2 x 25 mg/kg i.p. for 6 weeks. - MECHANISM OF ACTION - Prolyl-4-hydroxylase inhibitor; Collagen biosynthesis inhibitor.
CN103432165A Controlled-release multifunctional veterinary iron supplementing injection and production process thereof The invention discloses a controlled-release multifunctional veterinary iron supplementing injection and a production process thereof. The controlled-release multifunctional veterinary iron supplementing injection comprises iron-dextrin, vitamin A, crystalline-state vitamin D3, vitamin E, an emulsifier Cremaphor and a food-grade antioxidant. The production method of the controlled-release multifunctional veterinary iron supplementing injection comprises the following steps of fully mixing the vitamin A with the vitamin D3 and the vitamin E at first, adding the emulsifier Cremaphor to the mixture after mixing, stirring the mixture in an emulsifying stirrer at the stirring temperature of 50 DEG C and the rotating speed of 45 r/min to obtain a homogeneous transparent solution, and then adding the iron-dextrin to the vitamin mixed solution for emulsification. The controlled-release multifunctional veterinary iron supplementing injection is simple in production process, has an obvious controlled release effect and a stable pesticide effect, and has no untoward effects such as allergy and stress.
EP2646040A1 Priming solutions for cardiopulmonary bypass The present invention relates to priming solutions used during cardiopulmonary bypass procedures. In particular, the present invention relates to a cardiopulmonary bypass priming solution comprising a balanced salt solution and a combination of oncotic and non-oncotic dextran molecules. The present invention also relates to the use of the priming solution in a cardiopulmonary bypass method, a method of maintaining oncotic pressure in a patient during a cardiopulmonary bypass procedure, and a combination of cardiopulmonary bypass priming solution and cardiopulmonary bypass apparatus.
US20120157543 Preparation of (r,r)-fenoterol and (r,r)-or (r,s)-fenoterol analogues and their use in treating congestive heart failure This disclosure concerns the discovery of (R,R)- and (R,S)-fenoterol analogues which are highly effective at binding β2-adrenergic receptors. Exemplary chemical structures for these analogues are provided. Also provided are pharmaceutical compositions including the disclosed (R,R)-fenoterol and fenoterol analogues, and methods of using such compounds and compositions for the treatment of cardiac disorders such as congestive heart failure and pulmonary disorders such as asthma or chronic obstructive pulmonary disease.
EP1547996A1 Diagnostic probes and remedies for diseases with accumulation of prion protein, and stains for prion protein A compound, which is used for the diagnosis and the prophylaxis/treatment of diseases in which prion protein is accumulated, or specific staining of abnormal prion protein in samples, represented by the formula (I) or (II):
EP2417974A1 Combination therapy for treatment of immune disorders Methods and compositions are provided for the treatment of immune disorders, such as autoimmune diseases, or cancers, involving combination therapy with agents that inhibit the development or maintenance of Th17cells. Treatment regimens are provided in which an antagonist of a pro-inflammatory cytokine is administered for a time sufficient to alleviate signs and symptoms of an acute phase flare-up of the autoimmune disease, or cancer, and treatment with an antagonist of IL-23 is continued for a longer time to prevent recurrence of the acute event. Antagonists of PGE2 and CD 161 are also disclosed for use in treatment of autoimmune, inflammatory and proliferative disorders.
CN103054825A Paliperidone derivative low-dose tablet and preparation method thereof The invention provides a paliperidone derivative low-dose tablet and a preparation method thereof. The paliperidone derivative low-dose tablet is prepared by using spray drying-lactose monohydrate as the diluent and filler by using a wet granulation method. Active components of extreme micro-quantity (can be as low as 0.375% of the weight of the materials) and other auxiliary materials are kept in very good uniform state in the mixing and wet granule preparation process; the defect that the spray drying-lactose monohydrate is poor in compressibility can be greatly overcome in the wet granulation process, so that the prepared granule is good in flowability and can be applied to direct compression so as to obtain the tablet with good content uniformity, hardness and friability results, and the tablet reveals excellent batch repeatability; and meanwhile the wet granulation method can greatly reduce the dust pollution degree in the whole production process, and reduces the influence to the health of operation personnel.
US6841543 Contacting a human immune cell with a sufficient amount of a pharmaceutical composition consisting essentially of non-crosslinked, monovalent Lewisx antigen consisting of LNFP-III lacto-N-fucopentaose III Methods for modulating immune responses are provided. The methods involve contacting an immune cell with an agent that modulates interaction of a compound comprising a Lewis antigen with the immune cell such that production by the immune cell of at least one cytokine that regulates development of a T helper type 1 or T helper type 2 response is modulated. In one embodiment, the agent is a stimulatory form of a compound comprising a Lewis antigen, such as a Lewisy, Lewisx or Lewisa oligosaccharide, or a derivative thereof. In another embodiment, the agent is an inhibitory form of a compound comprising a Lewis antigen, such as a Lewisy, Lewisx or Lewisa oligosaccharide, or a derivative thereof. In various embodiments, the immune cell is a human immune cell, a macrophage or a T cell. Pharmaceutical compositions for modulating immune responses are also provided.
EP1633712A2 Six membered amino-amide derivatives as angiogenesis inhibitors The present invention relates to six membered amino-amide derivatives, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability, to their use as medicaments and to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans.
EP1123414B1 Antisense modulation of integrin alpha 4 expression Compositions and methods are provided for modulating the expression of integrin α4. Antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding integrin α4 are preferred. Methods of using these compounds for modulating integrin α4 expression and for treatment of diseases associated with expression of integrin α4 are also provided.
US20080299196 Controlled Release Pharmaceutical Compositions Comprising a Fumaric Acid Ester The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designed to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects.
CN1720921A Antineoplastic medicinal composition, its preparation method and application Disclosed is an anti-tumor medicinal composition containing cardiac glycoside compound of forrestin A-3-O-beta-D-glucopyranose (1-4)-beta-D-Apocannoside or 3 beta,6 beta,14 beta-trihydroxy-8 beta-H-20 (22) lactone glycoside or periplogenin-3-O-beta-D-glucopyranose (1-4)-beta-D-Apocannoside as the active ingredients, and the conventional medicinal carrying agents. The invention also discloses the process for preparing the medicinal composition and the use in preparing medicament for treating tumors.
WO2005110490A8 Phospholipase c gamma modulation and uses thereof for management of pain and nociception The present invention provides methods of preventing and treating pain, by modulating, e.g. inhibiting, the activity, function and/or expression of a PLCϜ in a subject. The invention further relates to methods of identifying agents capable of modulating the activity and/or expression of a PLCϜ, or capable of modulating binding of a ligand or binding partner to a PLCϜ, and their use thereof for the prevention and/or treatment of pain. In a further aspect, the invention provides methods for the diagnosis and prognostication of pain by determining whether there is modulation of activity and/or expression of a PLCϜ, relative to a corresponding control.
WO2013100660A3 Pharmaceutical composition for treatment of eye pain, containing pge2 synthesis inhibitor The present invention relates to a pharmaceutical composition for the treatment of eye pain, containing a PGE2 synthesis inhibitor. The use of the pharmaceutical composition for the prevention or treatment of eye pain according to the present invention, which contains the PGE2 synthesis inhibitor as an active ingredient, makes it possible to alleviate the symptoms of eye pain by selectively inhibiting the PGE2 expression level, and also has the advantages of treating and preventing xerophthalmia and of overcoming and preventing eye discomfort caused by various inflammation-inducing circumstances including following surgery. Also, by using a kit for detecting the amount of PGE2, PGD2 and COX2, the present invention makes it possible to easily diagnose eye-pain symptoms in clinical practice, and can be widely used in checking the state not only of patients having xerophthalmia but also patients following eye surgery.
WO2007136116A2 C-phenyl glycitol compound for the treatment of diabetes Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, Y is a C1-6 alkylene group, -O-(CH2)n- (n is an integer of 1 to 4) or a C2-6 alkenylene group, provided that when Z is NHC(= NH)NH2 or -NHCON(RB)RC, n is not 1, Z is -CONHRA, -NHC(=NH)NH2 or -NHCON(RB)RC, Formula (A) or Formula (B).
CN103520126A Almotriptan tablet and preparation method thereof The invention provides an almotriptan tablet, which is prepared from the following raw materials and accessories by weight: 15-20 parts of malic acid almotriptan, 20-50 parts of mannitol, 20-50 parts of microcrystalline cellulose, 2-8 parts of sodium carboxymethyl starch and a proper amount of a lubricant. Through screening on the proportion of raw materials and accessories, the invention finally prepares the almotriptan tablet with good appearance shape and dissolution rate, and provides a new choice for clinical medication.
WO2008117282A1 Polymorph of granisetron base and production process therefor Provided is crystalline granisetron base form I and processes for producing crystalline granisetron base form I, which is suitable for preparing, e.g., granisetron salts such as, e.g., the hydrochloride salt. Also provided is a process for producing a salt of granisetron from crystaline granisetron base form (I).
US20110201652 2,4-Disubstituted Pyrrolidine Orexin Receptor Antagonists The present invention is directed to 2,4-disubstituted pyrrolidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
US20090149470 aurora kinase inhibitors; 2-(thiazol-2-ylamino)pyridine compounds as antitumor agents; 6-((4-(3-chloro-2-fluorobenzoyl)piperazin-1-yl)methyl)-N-thiazol-2-ylpyridin-2-amine for example The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is hydrogen atom, etc. and Rbj and Rbj′ is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).
US7629324 Antisense oligonucleotides for treating atopic diseases and neoplastic cell proliferation The present invention relates to the use of antisense oligonucleotides directed against specific nucleic acid sequences coding for receptors, alone or in combination, in order to inhibit the inflammatory reaction that is present in asthma, atopy or hypereosinophilia and to inhibit neoplastic cell proliferation. The antisense oligonucleotides of the present invention are used for treating and/or preventing asthma, allergy, hypereosinophilia, general inflammation or cancer. The oligonucleotides of the present invention are more specifically directed against nucleic acid sequences coding for a CCR3 receptor, a common sub-unit of IL-4 and IL-13 receptors, or a common sub-unit of IL-3, IL-5 and GM-CSF receptors.
US20120065259 Heat assisted lidocaine and tetracaine for transdermal analgesia The present disclosure is drawn to methods for treating various types of pain, including pain associated nerve entrapment, neuroma, headaches, connective tissue, arthritis, injury, and/or overuse. Specifically, the method includes the application of an analgesic system to a skin surface of a subject experiencing the pain and maintaining the analgesic system on the skin surface for an application period of at least 30 minutes. Following the application period the analgesic system can be removed and the subject being treated continues to experience reduction of pain for a period of 2 to 10, or even 4 to 12 hours after removal of the analgesic system. The analgesic system applied to the skin surface can include a heating component and a local anesthetic formulation.
CN101524475A Sheep ossein tendon-and-bone strengthening calcium for preventing fatigue and tonifying kidney The invention relates to the filed of homology of medicine and food made from animal and plant life, in particular to a preparation method of sheep ossein tendon-and-bone strengthening calcium for preventing fatigue, tonifying kidney, promoting vital essence and blood generation, supplementing calcium and vitamins and increasing bone density. In the invention, after sheep bone, cornu cervi degelatinatum, ass bone, mother of pearl, dragon bone and radix pseudostellariae are mixed, alcohol extracts are respectively carried out for twice, the extract is combined, condensed and dried to prepare dry paste for standby use; the leavings, prepared rhizome of rehmannia, sealwort, medlar, niger seed and colla corii asini are respectively decocted and extracted with water twice, the extract is combined, condensed and dried to prepare dry paste. The two dry pastes are combined and then crushed into fine powder that is added with milk powder, milk sugar, cane sugar, milk sugar, dextrine, flavor composition, vegetable fat powder, protein honey, starch, calcium lactate, calcium gluconate and vitamin to prepare granules in terms of bags, or tablets, oral liquid, and the like.
US20110195942 Method of making and using 7alpha, 11beta-dimethyl-17beta-hydroxyestr-4-en-3-one 17-undecanoate Methods of using 7α,11β-dimethyl-17β-hydroxy-4-estren-3 -one bucyclate (I) and 7α,11β-dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate (II) for various hormonal therapies, dosage forms comprising 7α,11β-dimethyl-17β-hydroxy-4-estren-3-one bucyclate and 7α,11β-dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate, and processes for their preparation.
CN1938294A Novel pyrrolidine-3,4-dicarboxamide derivatives The invention is concerned with novel pyrrolidine-3,4-dicarboxamide derivatives of Formula (I) ; wherein R to R and X are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
US20110251280 Stable Aqueous Compositions Comprising Amide-Protected Bioactive Creatine Species and Uses Thereof The present invention provides amide-protected creatine molecules and compositions, containing one or more bioactive forms of creatine in aqueous compositions, wherein bioactive forms of creatine do not appreciably degrade into creatinine. Also provided are various beneficial effects of administering aqueous compositions having at least one amide-protected creatine molecule.
WO2013191187A1 Adhesive preparation composition obtained by blending drug, organic solvent, lipophilic ointment base, and powder The purpose of the present invention is to provide a slow-releasable, non-aqueous skin patch composition of favorable adhesive strength. The addition of a powder component (a filler or the like) allows this skin patch to achieve improved adhesive strength of the skin patch and improved release of the drug. As a result, the adhesive strength of the skin patch is maintained for a long time, thereby making it possible to improve percutaneous absorption and enable slow release. The use of the skin patch composition containing this powder component causes a drug, regardless of the type of drug, to be dissolved into an organic solvent or ionic liquid and to be incorporated into the non-aqueous skin patch as a principal drug solution along with the organic solvent, thereby realizing a preparation of both improved percutaneous absorption and improved slow release.
US8679503 Methods, compositions and kits relating to chitnases and chitnase-like molecules and inflammation disease The present invention includes compositions and methods for the treatment of inflammatory disease (e.g., asthma, COPD, inflammatory bowel disease, atopic dermatitis, atopy, allergy, allergic rhinitis, scleroderma, and the like), relating to inhibiting a chitinase-like molecule. The invention further includes methods to identify new compounds for the treatment of inflammatory disease, including, but not limited to, asthma, COPD and the like. This is because the present invention demonstrates, for the first time, that expression of IL-13, and of a chitinase-like molecule, mediates and/or is associated with inflammatory disease and that inhibiting the chitinase-like molecule treats and even prevents, the disease. Thus, the invention relates to the novel discovery that inhibiting a chitinase-like molecule treats and prevents an inflammatory disease.
US20090318403 Antibiotic composition The present invention provides antimicrobial compositions comprising an antibiotic and a sensitizer that enhances the effectiveness or activity of the antibiotic, wherein the sensitizer is preferably a primary amine containing a long alkyl chain. Such compositions are particularly useful for the treatment of infections by drug resistant bacteria.
CA2186044C Novel mutated viruses, anti-viral compounds and novel methods of making vaccines The present invention provides a composition of matter, comprising a non-infectious, mutated virus suitable for use in preparing a vaccine. A plasmid adapted for expression in a recombinant cell comprising DNA encoding non-infectious mutated virus protein and regulatory elements necessary for expression of said DNA in the cell. Also provided are methods of inhibiting the spread of infection of a virus comprising the step of contacting said virus with a compound that inhibits thiol-reductase/protein disulfide isomerase activity in said virus.
WO2010131865A2 Antimicrobial composition with an activity against an antibiotic-resistant strain The present invention relates to an antimicrobial composition against an antibiotic-resistant strain containing, as active ingredients, one or more elements selected from a group consisting of sulforaphene and sulforaphane. More particularly, the present invention relates to an antimicrobial composition which contains, as active ingredients, one or more elements selected from a group consisting of sulforaphene and sulforaphane, and which acts on methicillin-resistant staphylococcus, vancomycin-resistant enterococcus or antibiotic-resistant colon bacillus, pneumobacillus, salmonella typhimurium and enterococcus faecalis and the like to inhibit the growth of an antibiotic-resistant strain. The antimicrobial composition of the present invention inhibits the growth of gram-negative bacillus and gram-positive bacillus having a resistance to beta-lactam antibiotics such as vancomycin, penicillin, methicillin and the like or against non-beta-lactam antibiotics, and therefore can be used in the prevention and treatment of various infectious diseases caused by antibiotic-resistant bacterial infections, and can be valuably used as antibiotics against super-bacteria.
EP1051179B1 Anti-estrogen plus progestin containing oral contraceptives This invention provides a method of providing contraception which comprises administering to a female of child bearing age a combination of a non-uterotrophic anti-estrogen and a progestin for 28 days per 28-day menstrual cycle.
CN103463183A Medicament for treating pulmonary infectious diseases and application thereof The invention discloses a medicament for treating pulmonary infectious diseases and an application thereof, which belong to the technical field of medicaments. The medicament comprises any substance or a composition of more than two substances of total flavonoids extracted from elsholtzia blanda or calamint, neohesperidin dihydrochalcone, naringin dihydrochalcone, 7-methoxy wogonin, 6,7-dimethoxy wogonin or pharmaceutically acceptable salts thereof. The invention provides the medicament for treating the pulmonary infectious diseases on one hand, the medicament has such pharmacologic actions as anti-virus, inhibition of virus induced lung injury, pulmonary edema and pneumonia, and reduction of bronchial mucus secretion and the like, and on the other hand, the invention determines the application of the medicament in treating the pulmonary infectious diseases; the medicament can be used for treating acute pneumonia, viral pneumonia, pulmonary edema or bronchitis.
WO2011010715A1 Pr-set7 inhibitor Disclosed is an inhibitor for histone methyltransferase Pr-Set7, which contains a compound represented by formula (I), (II) or (III), a salt thereof or the like, and which is useful as an active ingredient for pharmaceutical products that are used for prevention and/or treatment of cancers or lifestyle-related diseases. (In formula (I), R1 and R2 each represents an alkyl group or the like; R3, R4 and R5 each represents a hydrogen atom or the like; and Ar represents a phenyl group or the like. In formula (II), R11, R12, R13, R14, R15, R16 and R17 each independently represents a hydrogen atom or the like; and X represents a phosphorus atom or the like. In formula (III), R21, R22 and R23 each independently represents a hydrogen atom or the like; and R24 and R25 each independently represents a C3-6 alkyl group or the like.)
US20050080255 Reacting cefdinir with potassium compound; salt formation; crystallization from solvent The present invention relates to a novel crystalline cefdinir potassium dihydrate, to a process for its preparation and to a method of preparing pure cefdinir via the crystalline salt.
WO2010018856A1 Prophylactic/ameliorating or therapeutic agent for cannabinoid receptor-related disease Disclosed is a prophylactic/ameliorating or therapeutic agent for CB receptor-related diseases, which comprises at least one member selected from the group consisting of ω3PUFAs and pharmaceutically acceptable salts and esters thereof as an active ingredient. Also disclosed is a method for utilizing the prophylactic/ameliorating or therapeutic agent. It becomes possible to provide a safe and highly effective prophylactic/ameliorating or therapeutic agent for CB receptor-related diseases and a method for utilizing the prophylactic/ameliorating or therapeutic agent.
WO2012136873A8 Triazine derivatives and their uses as trpv1 inhibitors The invention relates to triazine-derived compounds, having the capacity to block TRPV1 and the therapeutic and cosmetic uses thereof. More specifically, the authors of the invention have synthesized trisubstituted triazines which are capable of specifically inhibiting the TRPV1 thermoreceptor in its activated state.
CN102786447A N,N-disubstituted aryl sulfonamide compound as well as preparation method and purpose of N,N-disubstituted aryl sulfonamide compound The invention belongs to the technical field of chemical medicine, in particular to a N,N-disubstituted aryl sulfonamide compound as well as a preparation method and a purpose of the N,N-disubstituted aryl sulfonamide compound. The N,N-disubstituted aryl sulfonamide compound has a structure shown by a formula I. The synthesized N,N-disubstituted aryl sulfonamide compound can inhabit the generation of beta-amyloid protein, in addition, the goal of treating alzheimer diseases and traumatic brain injury can be reached through inhabiting the activity of gamma-protein secretase and beta-protein secretase in the beta-amyloid protein generation process, and a new choice is provided for the development of medicine for treating alzheimer diseases and traumatic brain injury.
WO2014022879A1 Compounds for the treatment of mtor pathway related diseases The present invention relates to compounds for the treatment of mTOR (mammalian Target Of Rapamycin) pathway related diseases. Specifically, the present invention relates to the use of aminoactonitrile derivatives (AADs) in the treatment of mTOR pathway related diseases.
CN101601668A Application of thiophene compound The invention provides application of a thiophene compound in preparing medicaments for resisting tumors. The tumors comprise cerebroma, lung cancer, liver cancer, mammary cancer, prostatic cancer, pancreatic cancer, cervical cancer, stomach cancer, esophageal cancer and the like. The results of screenings on anti-tumor actions and cancer chemical prophylaxis performed by an MTT method show that the thiophene compound is concentration-dependent to inhibit the multiplication of tumor cells and can remarkably induce the expression of quinone reductase; and the results of a research on anti-inflammatory actions performed by a Westernblot method show that the thiophene compound can remarkably inhibit the expression of NFkappaB. The thiophene compound can also be applied to preparing cancer chemical prophylaxis medicaments, anti-inflammatory medicaments and the medicaments for inhibiting the generation of tumor vessels.
US20060111309 Chalcomycin derivatives The invention relates to novel chalcomycin derivatives, medicaments containing said derivatives or the salts thereof, and the use of chalcomycin derivatives for treating diseases, especially infections. The inventive chalcomycin derivatives are acylated on the sugar esters and derivatives are also acylated on the 9-carbonyl function.
WO2006074117A3 Silver/water, silver gels and silver-based compositions; and methods for making and using the same We disclose a colorless composition comprising metal particles (e.g., silver nanoparticles) and water, wherein said particles comprise an interior of elemental metal (e.g., silver) and an exterior of metal oxide (e.g., one or more silver oxide(s)), wherein the metal nanoparticles are present in the water at a level of about 5-40 ppm, and wherein the composition manifests significant antimicrobial properties. Methods of use of the composition are described. The composition can be incorporated into a hydrogel with essentially no loss of antimicrobial properties. Various metal-containing compositions with unexpected biological efficacy are also disclosed.
US20080089948 Method of use for lanthanum carbonate and lanthanum hydroxycarbonate A method for treating hyperphosphatemia using lanthanum carbonate, including analytically determining the amount of an impurity in the lanthanum carbonate sample is provided. This X-ray diffraction method preferably uses the Rietveld refinement.
US20120065151 Substances Mixture, Use and Infusion Solution The present disclosure relates to a substance mixture, wherein the substance mixture contains ribose, alanine, nicotinic acid and ascorbic acid.
US20130052152 Protective wound dressing device for oral and pharyngeal space The present invention provides a wound dressing comprising a tessellated water-soluble molding matrix comprised of a polymer selected from the group consisting of polyvinyl alcohol, gelatin, and mixtures thereof and a 1,1-disubstituted ethylene monomer. The present invention further provides methods of using the wound dressing and kits containing the wound dressing.
WO2012142080A1 Thioamide, amidoxime and amidrazone derivatives as hiv attachment inhibitors A compound of Formula (I), including pharmaceutically acceptable salts thereof: wherein A is selected from the group of Formula (A1), (A2), (A3), (A4) and (A5).
EP0824530B1 Aryl glycinamide derivatives, methods of producing these substances and pharmaceutical compositions containing such compounds The invention concerns novel aryl glycinamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof, the symbols having the following meanings: R?1 and R2¿ together with the nitrogen atom to which they are bound form a ring of formula (II) shown in which p is 2 or 3 and X stands for oxygen, N(CH¿2?)nR?6 or CR7R8; and R3, R4, R5, R6, R7, R8¿, Ar and n have the meanings indicated in the description. The invention also concerns the production and use of these substances. The novel compounds are valuable neurokinin (tachykinin) antagonists.
EP1143950B1 Topical application products against onychomycoses The invention relates to water-free topical application products for the treatment of nail diseases and nail care, containing one or more C1-C4-alkyl esters of lactic acid, malic acid, tartaric acid or citric acid as carriers in addition to one or more active substances and optionally physiologically compatible adjuvants. The products disclosed in the invention are also suitable for the treatment of mycotic infections of the hooves, paws and claws of pets and domestic animals in veterinary medicine.
CA2360451C N-[2-hydroxy-3-(1-piperidinyl)propoxy]pyridine-1-oxide-3-carboximidoyl chloride and its use in the treatment of insulin resistance The invention relates to N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl chloride, its stereoisomers and the acid addition salts thereof, pharmaceutical compositions containing the same, the use of these compounds in the treatment of pathological insulin resistance, and for the treatment of pathological conditions associated therewith, for the treatment of pathological insulin resistance, and the treatment of pathological conditions associated therewith, by simultaneous treatment and prevention of diabetes-induced chronic complications, especially retinopathy, neuropathy and nephropathy and/or with simultaneous increasing pathologically decreased peripheral neuroregeneration caused by diabetes and methods of treatment.
US7972630 Injectable bone mineral substitute material An injectable bone mineral substitute material composition comprises an inorganic bone cement powder and a biologically compatible oil. The oil is an intermixture with the cement powder at a concentration of less than 10 wt % of the total weight of the composition in order to improve the rheology of the same. In a method of intermixing a powder of an implant material and a biologically compatible oil to a composition the oil is mixed with the powder of implant material at an elevated temperature.
US20060217379 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.
CN102626423A Compound preparation containing heptaene menadione and application thereof The invention provides a compound preparation containing heptaene menadione. The compound preparation comprises heptaene menadione, vitamin D, a calcium agent and a solid substrate or an oily substrate, wherein the heptaene menadione is extracted from a natural product or synthesized artificially. Every kilogram of the compound preparation contains 0.1-1g of heptaene menadione, 0.008-0.02g of vitamin D and 100-300g of element calcium in the calcium agent. In the compound preparation provided by the invention, calcium and vitamin D3 play important roles in an anti-osteoporosis mechanism, side effects existing in the conventional medicament for treating osteoporosis are effectively avoided by using the unique regulating and controlling mechanisms of heptaene menadione with high safety and high activity in calcium and bone metabolism, and the defects of unremarkable effect and possibility in causing hypercalcemia existing in a high-dose calcium-vitamin D health-care preparation are overcome. The invention further provides an application of the compound preparation to the preparation and treatment of middle-aged and old and postmenopausal women osteoporosis.
US20100261664 Novel heterocyclic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof Novel heterocyclic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof The invention relates to substituted heterocyclic fluoroglycoside derivatives of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation. The compounds are suitable for example as antidiabetics.
US20100034798 Composition and method of use for intestinal health Therapeutic compositions can include ingredients to be useful in methods for improving or maintaining proper intestinal health. The therapeutic compositions can be used for maintaining a healthy intestinal tract by providing essential nutrients for intestinal function. Also, the therapeutic compositions can improve intestinal health by providing functional ingredients that can be useful for returning the intestinal tract to a healthy condition for optimal performance. The therapeutic compositions can be beneficial for small and large intestines, and other aspects of the GI tract as well as for the general heath of an individual.
CA2587749A1 Piperidine derivative and process for producing the same A piperidine derivative represented by the formula (I) or a salt thereof is used as an intermediate. Due to this, a 2-cyano-4-fluoropyrrolidine derivative useful as a medicine, especially a DPP-IV inhibitor, can be efficiently produced. In particular, use of the intermediate enables the target compound to be produced through a smaller total number of steps than in conventional processes and improves the overall yield. The 2-cyano-4-fluoropyrrolidine derivative can be produced without using an ultralow-temperature reaction or a reaction necessitating strict control of water in the reaction system, which are unsuitable for industrial production. (I) [In the formula, Ms represents methanesulfonyl, Me represents methyl, and R1 represents -H, halogeno, or -OH.]
US20100080760 Method, device, and system to control pH in pulmonary tissue of a subject Methods, devices, and systems are provided which include an aerosol generator and a pharmaceutical composition including a membrane selective for a charged ion configured to achieve a selected pH of a pulmonary tissue in a subject. The methods, devices, or systems which include the membrane may be configured to alter selectivity for the charged ion in response to a sensed condition in the pulmonary tissue.
CN102727581A Pharmaceutical composition with wound repairing effect The invention discloses a pharmaceutical composition with a wound repairing effect. The active ingredients of the pharmaceutical composition comprise, by weight: 2g-8g of chitosan oligosaccharides, 0.5g-2g of Salvia Miltiorrhiza, 0.2g-1g of Angelica, and 0.5g-1.3g of folium artemisiae argyi. The pharmaceutical composition is applied to wound repairing tests, and results show that wounds generally heal, and no obvious scar is left. Cell proliferation tests prove that the pharmaceutical composition has good proliferation and regeneration functions on cells. After acute toxicity tests of the pharmaceutical composition performed by the inventor of the invention, the tested pharmaceutical composition can be judged non-toxic according to acute toxicity grading standards. Therefore, the pharmaceutical composition of the invention can be used for treating bedsores, normal wound healing, surgical wound healing, burns, and scalds, and boasts a great clinical value.
EP1655382A2 Colon specific gene and protein Human colon specific gene polypeptides and DNA (RNA) encoding such polypeptides and a procedure for producing such polypeptides by recombinant techniques is disclosed. Also disclosed are methods for utilizing such polynucleotides or polypeptides as a diagnostic marker for colon cancer and as an agent to determine if colon cancer has metastasized. Also disclosed are antibodies specific to the colon specific gene polypeptides which may be used to target cancer cells and be used as part of a colon cancer vaccine. Methods of screening for agonists and antagonists for the polypeptide and therapeutic uses of the antagonists are also disclosed.
CN1732950A Composition of cefuroxime sodium and tazobactam sodium for injection The invention provides a composition of cefuroxime sodium and tazobactam sodium for injection, which comprises cefuroxime sodium and tazobactam sodium by a weight ratio of 3:1 or 5:1. These compositions have better antibiotic action.
US20090060853 Aminophenylbenzothiazole compounds The Use, as a UV filter, of a compound of formula R1 and R2 are each independently of the other hydrogen; unsubstituted or halo-, amino-, mono- or di-C1-C5alkylamino-, cyano- or C1-C5alkoxy-substituted C1-C22alkyl, C5-C10cycloalkyl, carboxy-C1-C22alkyl, carboxy-C6-C10aryl, C6-C10aryl, C6-C10aryl-C1-C5alkyl; carbamoyl; or sulfamoyl; or R1 and R2, together with the nitrogen atom linking them, form a 5- to 7-membered heterocyclic radical; and R3 is hydrogen; or C1-C22alkyl; and R4 is hydrogen; hydroxy; C1-C22alkyl; or C1-C22alkoxy; is described. The compounds of formula (1) are suitable especially as UV filters in cosmetic preparations.
US20120058184 Formulations and uses of 2-hydroxy-5-phenylazobenzoic acid derivatives for the treatment of males The instant application provides methods and compositions for the treatment of male subjects having ulcerative colitis.
CN103656098A Composite fish oil soft capsule and preparation method thereof The invention relates to a composite fish oil soft capsule and a preparation method thereof. The composite fish oil soft capsule consists of a soft capsule body and contents in the soft capsule and is characterized in that the composite fish oil soft capsule is obtained by weighing 38-62 percent of fish oil, 3-5 percent of vitamin E, 4-8 percent of a grape seed extract, 6-10 percent of a ginkgo biloba extract, 15-25 percent of garlic oil, 5-7 percent of beewax and 5-7percent of lecithin in percentage by weight, uniformly mixing, grinding and degassing the materials to obtain the contents in the soft capsule, weighing gelatin, water and glycerinum according to the ratio of 100:100:40, heating the materials to evaporate the materials, the performing degassing to obtain a capsule body filtrate, conveying the capsule body filtrate and the contents in the soft capsule according to the ratio of 1: (2-4) into a ball pressing machine for ball pressing, and performing sizing, drying, washing, sorting and packaging to obtain finished products. The composite fish oil soft capsule has reasonable components, is scientific in dosage and has functions of resisting oxidization and adjusting three highs. The preparation method for the composite fish oil soft capsule is reasonable in technology, high in operability and favorable for implementation of large-scale production.
WO2005030752A1 8-cyanoquinolonecarboxylic acid derivative A quinoline antibacterial which has potent antibacterial activity against gram-positive bacteria and gram-negative bacteria and is highly safe; and a therapeutic agent for infectious diseases. Provided is a compound represented by the following formula (1): (Chemical formula 1) (wherein R1 represents optionally substituted C3-6 cycloalkyl, etc.; R2 represents hydrogen, etc.; R3 and R4 each independently represents hydrogen, C1-6 alkyl, or substituted carboxy derived from an amino acid, dipeptide, or tripeptide, provided that when R3 and R4 are C1-6 alkyl, then the alkyls each may be substituted by one or more atoms or groups selected among hydroxy, halogeno, C1-6 alkylthio, and C1-6 alkoxy; and n is an integer of 1 to 3), a salt of the compound, or a hydrate of either.
CN101899057A Preparation method of pyrimido-oxazole derivative and use thereof in medicine The invention relates to a synthetic method of a pyrimido-oxazole derivative which is related to inhibition of tumor angiogenesis and a medical use thereof. The preparation comprises the steps of taking 2-methyl-4,6-dichloro-5-aminopyrimidine as a starting raw material, and carrying out three-step reaction of N-alkylation condensation, acylation and ring-closing reaction. The method has simple operation, mild reaction conditions, cheap and readily-available raw materials and reaction reagents and high yield in each step. The compound is mainly applied in the inhibition of the tumor angiogenesis.
CA2354148C Aerosol formulations for buccal and pulmonary application A mixed micellar aerosol pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an alkali metal lauryl sulphate, at least three micelle forming compounds, a phenol and a propellant. The micelle forming compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linoleic acid, linolenic acid, monoolein, monooleates, monolaurates, borage oil, evening of primrose oil, menthol, trihydroxy oxocholanyl glycine and pharmaceutically acceptable salts thereof, glycerin, polyglycerin, lysine, polylysine, triolein, polyoxyethylene ethers and analogues thereof, polidocanol alkyl ethers and analogues thereof, chenodeoxycholate and deoxycholate. The amount of each micelle forming compound is present in a concentration of from 1 to 20 wt/wt.% of the total formulation, and the total concentration of micelle forming compounds are less than 50 wt./wt.% of the formulation. The propellant, e.g., a fluorocarbon propellant, provides enhanced absorption of the pharmaceutical agent, particularly in the buccal cavity.
US6916923 Method for synthesizing pyrazolobenzodiazepines Disclosed is a novel method for synthesizing pyrazolobenzodiazepines of formula I using intermediates of formula Pyrazolobenzodiazepines of formula I are useful in the treatment and control of solid tumors.
WO2013067881A1 Water-soluble vitamin e derivative-modified amphiphilic anticancer medicament compound and preparation, method for preparing the compound, and application thereof Disclosed is a water-soluble vitamin E derivative-modified amphiphilic anticancer medicament compound having a structure as represented by formula (I) or formula (II). An anticancer medicament active moiety, camptothecin or a camptothecin derivative, and an amphiphilic moiety, and water-soluble vitamin E alkoxy polyethylene glycol ester or amide, are covalently bonded via a linking group to form the amphiphilic anticancer medicament compound. The present invention also relates to a preparation of the medicament compound, a method for preparing same, and an application thereof.
CN102805749A Dispersible tablet comprising clopidogrel and aspirin The invention relates to a novel dispersible tablet, which consists of 37.5-300mg of clopidogrel or a pharmaceutically-acceptable salt thereof, 37.5-325mg of aspirin and at least one pharmaceutically-acceptable carrier, wherein the clopidogrel or a pharmaceutically-acceptable salt thereof is clopidogrel, clopidogrel bisulfate, clopidogrel hydrochloride, clopidogrel besylate or clopidogrel resinate. The novel dispersible tablet is used for preventing, delaying progress or treating acute coronary syndromes, angina and cardiovascular or cerebrovascular systemic diseases of patients. Compared with an ordinary tablet or capsule, the dispersible tablet has the characteristics of rapid and uniform dispersion, short disintegration time, quick medicament absorption, high bioavailability, high stability and convenience in taking.
CN102247462A Prescription for treating extremity ulcer The invention aims at providing a prescription for treating extremity ulcer. The prescription comprises the following materials: 10 grams of calaminae, 10 grams of rhizoma coptidis from Sichuan of China, 12 grams of ossa draconis, 12 grams of cortex phellodendri, 12 grams of rheum officinale, 10 grams of lithodes, 5 grams of leaching monoxide and 3 grams of cinnabar.
WO2011146618A1 Inhibitors of human 12-lipoxygenase Disclosed are inhibitors of human 12-lipoxygenase of Formula (I) or (II), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating or preventing a 12-lipoxygenase mediated disease or disorder, e.g., diabetes. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal.
US20120122938 Alkoxy Compounds for Disease Treatment The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
CN102233000A Meizugao external ointment and preparation method thereof The invention provides Meizugao external ointment and a preparation method thereof. The Meizugao external ointment has the characteristics of instant effect and high cure rate. A manufacturing procedure of the ointment is as follows: preparing materials according to a corresponding proportion, adding the materials into a stainless steel mixer for ten-minute clockwise stir and fifteen anticlockwise stir, adding an adjustment agent and carrying out uniform mixing, followed by cooling for two minutes and bottling. The proportion of the materials is as follows: 0.1% of white Vaseline, 0.03% of liquid paraffin, 0.02% of glycerin, 0.02% of purified water, 0.01% of eleaostearic acid, 0.2% of borneol, 0.2% of methyl salicylate, 0.3% of synthetic camphor, 0.2% of menthol, 0.02% of 20-dione21-acetate, 0.1% of urea, 5% of beclomethasone propionate and 2% of merphenyl nitrate.
WO2007076104A1 Vanilloid receptor ligands and their use in treatments Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
US20120014947 Methods and compositions to reduce liver damage associated with conditions or therapies that affect the immune system One side-effect arising from the use of antibodies against TNF receptor family members as therapeutics can be liver damage which precludes the completion of clinical trial. A novel LT-dependent pathway is described that mediates liver cell injury in several disease models.
CN101503448A Nucleic acid molecule CXSI22 and use thereof in anti-cancer medicine preparation The invention belongs to the field of biological medicine and relates to a nucleotide molecule and the application thereof in the preparation of antineoplastic medicine. The invention provides a nucleotide molecule used for preparing the antineoplastic medicine, which has the activity of inhibiting tumor growth and the sequence including 5'-UAUUGCAAGAGCGACACAU-3' or 5'-TATTGCAAGAGCGACACAU-3'. The nucleotide molecule is called as CXSI22. The nucleotide molecule CXSI22 can stop the cell in the stage of G1 and can obviously inhibit the tumor growth when being applied to a nude mouse compared with a nude mouse under the same condition of culture.
CN102670668A Nutritional health-care product for regulating autonomic nerve The invention relates to the technical field of health-care medicaments and food, and in particular relates to a nutritional health-care product for regulating autonomic nerve. The nutritional health-care product for regulating autonomic nerve comprises glutamic acid fermentation broth, plant red algae calcium, vitamin B6 and vitamin B12 in a certain ratio, wherein the glutamic acid fermentation broth contains rich gamma-amino butyric acid (GABA) and is blended with other nutritional components, so that the cranial nerve can be relaxed, the pressure resistance is increased, nerve excitement is effectively reduced, effects of relieving pressure and relaxing emotion are achieved, the sleeping quality can be improved, symptoms such as mental stress, anxiety and insomnia caused by the autonomic nerve imbalance are effectively relieved, and the nutritional health-care product has good relieving and health-care treatment effects on the autonomic nerve imbalance. By adopting purely natural green materials, the nutritional health-care product has a remarkable effect, is safe, does not have any toxic or side effect, and has a certain health-care treatment effect on diseases caused by the autonomic nerve imbalance by long-term administration.
US20120252902 Treatment of adhd A method is provided for treating a subject in need of therapy for attention deficit hyperactivity disorder (ADHD) and related CNS disorder symptoms of impaired learning, impaired planning, impaired problem solving, impulsiveness attention deficit and aggression comprising administering to said subject an amount of a ketogenic material sufficient to produce a ketosis in the subject sufficient to provide therapeutic benefit in such behavioural disorders. Preferred materials produce a ketosis is such that the total concentration of acetoacetate and (R)-3-hydroxybutyrate in the blood of the subject is raised to between 0.1 and 30 mM.
CA2311128C Composition with azelaic acid The invention relates to a pharmaceutical composition that has the following components: azelaic acid, polyacrylic acid, triacylglycerides, propylene glycol, polysorbates, soybean lecithin, water and salts. The composition is a hydrogel, which is suitable for treatment of rosacea, presbyderma, melasma or skin irritations.
WO2013167403A1 Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors Substituted 6-(4-Hydroxy-phenyl)-l H-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula, in which R', R2 , R3, R4, R5 and R6 are defined as indicated below. The compounds of the formula I are proteine kinase C (PKC) inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
CN103169696A Use of effective components of Clausena lansium for treating neurodegenerative diseases The invention discloses use of effective components of Clausena lansium for treating neurodegenerative diseases. The effective components seven carbazole alkaloids of Clausena lansium (lour.)skeels are shown in the specification. The invention further discloses a preparation method of the seven carbazole alkaloids as well as application thereof in preparing medicines for treating neurodegenerative diseases, in particular stroke or stupid.
CN101269018A Leflunomide sustained-release dropping pills and preparation method thereof The invention discloses a medicine composition used for curing rheumatoid arthritis. The invention aims at making up the deficiency of the existing oral medicine (leflunomide troche) used for curing rheumatoid arthritis, and provides a leflunomide sustained-release pill that has the advantages of high bioavailability, rapid effect, high medication content, enough medicine release, controllable medicine release, few times needed by the patient to take the medicine, convenient medicine taking, low price and no pollution in the production. The leflunomide sustained-release pill related by the invention takes leflunomide as raw material and can be prepared together with medicated carrier that takes hydrophilic framework material and hydrophobic framework material as stroma.
US7335687 Used to treat hypercholesterolemia, hyperlipemia, arteriosclerosis, mycoses, gallstones, hyperproliferative disorders, impaired glucose tolerance, or diabetes; aminocyclohexanol derivatives; e.g. N-(4-(4-[ethyl-(2-hydroxy-ethyl)-amino]-but-1-ynyl)-cyclohexyl)-N-methyl-4-trifluoromethyl-benzenesulfonamide The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
WO2013155375A1 Enhanced anti-influenza agents conjugated with anti-inflammatory activity Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti- influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.
WO2009081275A2 Antifolate compounds for the treatment of melanoma This invention relates to compounds of the formula X) or Xl) (X) (XI) wherein: each -R1, -R2 and -R3 is independently -Q1, -OH or -H, where at least one of -R1, -R2 and -R3 is not -H or -OH; each -R4 and -R5 is independently -Q2 or -H; each -Q1 is independently selected from: -F, -Cl, -RA, -ORA,-SH, -SRA, where each -RA is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; and each -Q2 is selected from: -F, -Cl, -RB, -ORB, -SH, -SRB, where each -RB is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; which are useful in the treatment of melanoma.
US8653091 Pyrid-2yl fused heterocyclic compounds, and compositions and uses thereof Fused heterocyclic compounds are provided according to formula 1a or 1b: where R1, R2, and R3 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
WO2012016708A1 Oral dosage form comprising dimebolin and donepezil The invention relates to oral dosage forms comprising dimebolin and donepezil and to processes for producing them.
EP1399153B1 Pharmaceutical composition comprising orlistat and a fatty acid or salt thereof The present invention relates to pharmaceutical composition. More particularly, the invention relates to a solid pharmaceutical composition comprising a) a solid pharmaceutically active compound which is solid at ≥37 °C and b) a fatty acid or a fatty acid salt or a mixture of a fatty acid and a fatty acid salt, characterized in that the constituents from a) and b) show a depression of their melting points to ≤37 °C upon contact with an aqueous solution.
EP2681211A1 Crystalline compound comprising tiotropium bromide The present invention refers to a crystalline compound comprising a mixture of a compound of formula (I ) (Tiotropium bromide) and propionic acid, or a hydrate thereof, wherein the molar ratio of the compound of formula I and the propionic acid is in the range of from 1:0.3 to 1 :0.7 and a process for obtaining the same.
WO2007067807B1 Tetracyclines for treating ocular diseases and disorders Methods and compositions are disclosed for treating a patient suffering from a condition associated with a retinal and/or choroidal disease or disorder of the eye involving endothelial cell dysfunction, especially vascular endothelial cells of the eye, and especially before or in the absence of neovascularization. The therapeutic method involves administering a tetracycline, an analog of tetracycline, or a chemically modified tetracycline (CMT) to a patient suffering from such conditions. Also provided are compositions and methods for reducing breakdown of tight junctions in vascular endothelial cells; reducing IL-1 α concentrations; and inhibiting IL-1 α-mediated matrix metalloproteinase activity in endothelial cells of the eye and surrounding tissues.
CN102558389A Low molecular weight carboxyl-reduced derivatives of fucosylated glycosaminoglycans and preparation method and applications of low molecular weight carboxyl-reduced derivatives The invention discloses low molecular weight carboxyl-reduced derivatives of fucosylated glycosaminoglycans (LCRG). The extent of carboxyl reduction is not less than 20%. Weight-average molecular weight of the LCRG is about 3000-20000Da, and monosaccharides comprise acetyl galactosamine (GalNAc), glucose (Glc) or glucuronic acid (GlcUA) and fucose (Fuc) or sulfates of fucose (shown as -OSO3-). The mole ratio of GalNAc, Glc (containing GlcUA), Fuc and -OSO3- is about 1: (1+-0.3): (1+-0.3): (3.0+-1.0). The LCRG is a potent human immunodeficiency virus (HIV) Type 1 entry inhibitor which acts on conserved regions and has the advantages of high activity against HIV Type 1, high therapeutic index and no-drug-resistance, and the LCRG can be used for preventing or curing HIV. The invention further provides a preparation method of the LCRG. The carboxyl-reduced derivatives of fucosylated glycosaminoglycans and medicinal compositions of the carboxyl-reduced derivatives can be prepared into injection agents, lyophilized powder or suppository and the like.
US20100209342 Apcdd1 inhibitors for treating, diagnosing or detecting cancer The invention provides, inter alia, methods for methods for treating cancer, compositions for treating cancer, and methods and compositions for diagnosing and/or detecting cancer. In particular, the present invention provides compositions and methods for treating, diagnosing and detecting cancers associated with APCDD1 overexpression.
WO2014066686A1 Brain targets for neurotrophic factors to treat neurodegenerative disease Provided are method of treatment with MANF. In certain embodiments, the invention provides a method of treating Parkinson's disease by administering MANF to the substantia nigra.
CN103536561A Sulbactam sodium composition freeze-dried powder for injection The invention provides a sulbactam sodium composition freeze-dried powder for injection, and belongs to the field of medicine and medicine preparation technology. The sulbactam sodium composition freeze-dried powder comprises following raw material ingredients, by weight, 7.26 to 9.17 parts of sulbactam sodium, 6.02 to 7.97 parts of chitosan nanoparticle, and 81.34 to 87.55 parts of injection water. Advantages of the sulbactam sodium composition freeze-dried powder are that: 1) the sulbactam sodium composition freeze-dried powder possesses excellent synergistic antimicrobial effect with sulbactam sodium, antibiotic sensitive rate of various bacteria on the sulbactam sodium composition freeze-dried powder is high; 2) stability of sulbactam sodium against beta-lactamase is increased, and in vivo distribution is excellent; 3) improvement of activity is capable of shortening medication cycle of patients, and reducing occurrence likelihood of adverse reaction caused by accumulation of sulbactam sodium; and 4) the chitosan nanoparticle can be used as a freeze-dried skeleton agent of the freeze-dried powder injection instead of mannitol so as to avoid active effects of mannitol on human bodies.
CN102584690A Pyridine-2-ketone compound, as well as preparation method and applications of pyridine-2-ketone compound The invention discloses a compound shown in a formula I, or medical salt, wherein definitions of all groups are shown in specifications. The invention further relates to a preparation method of the compound, pharmaceutical compositions containing the compound, as well as an application of the compound in preparing antiviral drug and antitumor drug.
CN101606939B Fat-soluble vitamin freeze-dried powder needle and preparation method thereof The invention discloses a fat-soluble vitamin freeze-dried powder needle and a preparation method thereof. The preparation method thereof comprises the following steps that vitamin A, vitamin D2, vitamin E and vitamin K1 which are difficult to being dissolved into water are added into accessory tween-80 and mannitol to prepare the freeze-dried powder needle by special technique; the accessory tween-80 conforms to the European standards or British standard; the dioxane does not excess 5.0, therefore, the use safety of the free-dried powder needle is improved and the stability of the product isobviously improved. The water content of the prepared fat-soluble vitamin freeze-dried powder needle is controlled to be 2%, which is far lower than the water content in the freeze-dried powder needle of the prior art; practices prove that the fat-soluble vitamin freeze-dried powder needle has obvious stability compared with the fat-soluble vitamin freeze-dried powder needle in the prior art, thecontents of all effective ingredients in the freeze-dried powder needle are not easy to loss, the freeze-dried powder needle can be preserved for longer period under the premise that the quality of freeze-dried powder needle is guaranteed.
US20090304615 Tricyclic compounds as melanogenesis modifiers and uses thereof A method of identification of tricyclic compounds (formula I) that control melanin synthesis (melanogenesis), and the use of such compounds and compositions thereof to modify (e.g., inhibit) melanin production are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to aberrant melanogenesis activity including by way of non-limiting example, hyperpigmentation and others.
CN101784523A Novel compounds, compounds that influence cellular vesicular systems, pharmaceutical compositions, and use thereof The present invention relates to compounds that are suitable for treatment of disease states and influence cellular vesicular systems, especially the formation and/ or function of lipid droplets, said compound having the general formula I (I) wherein X are each independently hydrogen, halogen, -C1-20-alkyl, -C2-20-alkenyl, -C2-20-alkinyl, -C5-6-cykloalkyl, aryl, aralkyl, adamantyl,_heterocyclic, hydroxyl, hydroxyalkyl, Or -N-(R1, R2) group; n is 0, 1, 2, 3, or 4; R1 and R2 may each be independently hydrogen, straight or branching alkyl, cyclo-alkyl, aryl, aralkyl, heterocyclic group, wherein each is un-substituted or halogen substituted; or R1 and R2 together with the nitrogen in between them form a 5 or 6 member ring; A is a single bond, -O-, -S-, -CH2-, or -NH-; Y is O or S; Z is O or S; R' and R'' are each independently methyl, ethyl, isopropyl, isobuthyl, sec- butyl or terc-butyl; with the restriction that: X(n) cannot all be fluorine, and A be a single bond, and Y, as well as Z be O, and R', as well as R'' be isopropyl, and R1 and R2 be hydrogen at the same time. The present invention further relates to pharmaceutical compositions comprising such compounds and to use of such compounds for treatment of disease states.
EP1882689A1 Tri- or tetra-substituted-3-aminopyrrolidine derivatives A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I): wherein R1 and R2 represent hydrogen atom, or the like; R3 represents an alkyl group containing 1 to 6 carbon atoms, or the like; R4 and R5 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R4 and R5 do not simultaneously represent hydrogen atom; or the substituents R4 and R5 together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R4 and R5 to form a spirocyclic structure with the pyrrolidine ring; R6 and R7 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R8 represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X1 represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):
CN1962612A Novel pregabalin crystal form and preparing method thereof The invention discloses a (S)-(+)-3-aminomethyl-5-methyl hexanoic acid crystal (Pregabalin), which is characterized by the following: treating epilepsy, nervous pain and wide anxiety; possessing excellent stability; fitting for large scale of production; using Cu-Ka irradiation for Pregabalin; displaying feature peak at 9.6(2), 12.4(7.1), 18.5(4.8), 20.0(4.4) and 23.4(3.8) diffracted by X-ray powder at 2 thita and d value as crystal gap distance.
US20120277259 Substituted benzofused derivatives and their use as vanilloid receptor ligands The present invention relates to substituted benzofused derivatives, which can be used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.
US7319148 Comprising reactive hydrazide function used as initial synthons for preparing compounds capable of inducing mutations or capable of inhibiting a DNA polymerase or a kinase The invention concerns novel nucleotide analogues comprising a reactive hydrazide function used as initial synthons for preparing compounds (formula I) capable of inducing mutations or capable of inhibiting a DNA polymerase or a kinase. The invention also concerns nucleic acids comprising said nucleotide and nucleoside analogues. Among such compounds, can be cited in particular the compound of formula (I)
US20130216523 Methods for Facilitating Diagnosis, Prognosis and Treatment of Cancer by Detecting HER1 Expression Methods are provided for facilitating the diagnosis of subjects with HER1-activated cancers. In addition, method of treating subjects with a cancer characterized as having high levels of activated HER1 are provided. Also provided are methods for determining or otherwise assessing the prognosis of an subject with a HER1-activated cancer. The methods include the analysis of samples for the presence or the absence of activated HER1 markers as indicated by HER1-HER1 homodimers, HER1 phosphorylation at position 1173, pan-phosphorylation of HER1 or associated molecules, or HER1-HER2 heterodimers. Activated HER1 measurements can be used to track a subject's response to a treatment regimen, predict the success of using a particular treatment regimen, determine the effects of a treatment regimen, or for categorizing a subject in order to create a homogenous group for a clinical trial.
CN101524365A Gel solution for treating gastric ulcer and gastrorrhagia The invention relates to a gel solution for treating gastric ulcer and gastrorrhagia. The gel solution is characterized in that carboxymethylcellulose sodium and other gels are compounded to form a solution substrate; and the medicament is carried with honey and sesame oil. The gel solution has the advantages that: 1, the solution can form a layer of protective film on the surface of stomach and duodenum, isolates the functions of stimulation and erosion of gastric acid, protease and food on an ulcer part, thereby accelerating rehabilitation and healing of the ulcer face; and 2, the solution has the function of hemostasis and has obvious hemostatic effect on gastrorrhagia.
WO2013089402A1 Composition comprising gypenoside extract of gynostemma pentaphyllum (thunb.) makino for treating or preventing type ιι diabetes, obesity, or hyperlipidemia The present invention provides a pharmaceutical composition or a health functional food for the treatment or prevention of obesity, type ΙΙ diabetes, or hyperlipidemia comprising, as an active ingredient, a gypenoside extract of Gynostemma pentaphyllum (Thunb.) Makino which includes at least one dammarane type triterpenoid soponin compound selected from the group consisting of gypenoside UL1, gypenoside UL2, gypenoside UL3, gypenoside UL4, gypenoside UL5, gypenoside UL6, gypenoside UL7, and gypenoside XLVIII.
CN103462976A Application of Incarviatone A in anti-tubercle bacillus medicaments The invention discloses application of Incarviatone A in preparation of anti-tubercle bacillus medicaments. According to the current situation that tuberculosis morbidity and mortality rise due to high tuberculosis morbidity and presence of multiple-resistant strains of tubercle bacilli at present, the Incarviatone A has obvious tubercle bacillus inhibiting activity and good application prospect as discovered. The application of the Incarviatone A in preparation of the anti-tubercle bacillus medicaments is made public for the first time, the skeleton type is completely novel and the Incarviatone A has an unexpectedly strong tubercle bacillus inhibiting activity, so the probability that other compounds give any revelation does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently made in prevention and treatment of tubercle bacillus infection.
WO2008053270A3 Use of an egfr antagonist for the treatment of glomerolonephritis The present invention relates to uses, methods and compositions for treating immune-mediated glomerulonephritis, such as crescentic glomerulonephritis. More specifically, the invention relates to the use of an EFGR antagonist or of an inhibitor of EGFR or HB-EGF expression for the treatment of said diseases.
CN1634059A Pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorphenamine maleates gel formulation and its preparing process The invention relates to a pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorphenamine maleates gel formulation and its preparing process, which is prepared from chlorpheniramine maleate, d-pesudoephedrine hydrochloride, Dextromethorphan Hydrobromide, and right amount of base material. The preparation is in the form of gel type oral form, children are willing to take the preparation, the preparation has good effects for controlling children's virus infection of upper respiratory tract and treating children's common cold.
WO2010146132A1 Sulfonamides and sulfamides as zap-70 inhibitors The invention relates to compounds of formula (I), wherein R1 to R6 and T0 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
US7235578 Used as cytotoxins for cancer therapy and as prodrugs for gene-directed enzyme-prodrug therapy and antibody-directed enzyme-prodrug theraphy The invention provides processes of preparing 3-substituted 1-(chloromethyl)- 1,2-dihydro-3H-[ring fused indol-5-yl(amine-derived)] compounds of formula (I) and its analogues, or a physiologically functional derivative thereof, (I), wherein A and B together may represent a fused optionally substituted benezene, naphthalene, pyridine, furan or a pyrrole ring, where the optional substituents are represented by Y; X is halogen or OSO2R, and W is selected from NO2, NHOH, N(R3)2NHR3, NHCO2R3, N(phthaloyl) or NH2, or W is further selected from the group (a), wherein J is selected from OH or H, and P is a group which is a substrate suitable for a nitroreductase or carboxypeptidase enzyme. The invention is also directed to the use of compounds of formula (I) prepared by the processes of the invention as cytotoxins for cancer therapy and as prodrugs for gene-directed enzyme-prodrug therapy (GDEPT) and antibody-directed enzyme-prodrug theraphy (ADEPT).
US20090221604 Thiazole Compounds and Their Use as PGD2 Antagonists A compound for use as a PGD2 antagonist is of structural formula [1] in which: A represents a fully saturated or partially unsaturated monocyclic 5-7 membered ring containing one or two nitrogen atoms; B represents a direct bond, an optionally substituted methylene group, an optionally substituted nitrogen atom, oxygen, or S(O)n, where n=0, 1, or 2; L represents a direct bond, or an optionally substituted alkylene or alkenylene group; R1 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; R2 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; X represents a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid or a group of formula C(═O)NHSO2Y or SO2NHC(═O)Y; and Y represents an optionally substituted aryl or heteroaryl group or an optionally substituted alkyl or cycloalkyl group; or a N-oxide, pharmaceutically acceptable salt, solvate or prodrug thereof.
US20120015023 Treatment of tumors prostate with arsonoliposomes The invention provides a method for treating a prostate proliferative disorder, such a prostate carcinoma or a begnin prostatic hyperplasia, in a patient, which method comprises administering arsonoliposomes comprising arsonolipids, wherein the arsonolipids are 2,3-diacyloxypropylarsonic acids, to a patient in need thereof.
CN102212148A Antithrombotic medicament for intravenous injection and preparation method and application thereof The invention provides an antithrombotic medicament for intravenous injection. The medicament is a modified acidic polysaccharide consisting of only one monosaccharide and has a structural general formula, wherein R is -CH3 or -CH2-CH(OH)-CH3; R' is -H or -SO3Na; each sugar ring has at least one R' which is -SO3Na; n is equal to 2 to 6; when R is -CH3, the compound represented by the structural general formula is an oligomannuronicacid methyl acetate sulfate sodium salt; and when R is -CH2-CH(OH)-CH3, the compound represented by the structural general formula is an oligomannuronicacid proply acetate sulfate sodium salt. The medicament for intravenous injection has obvious anticoagulation, wherein the anticoagulation titer is 17 to 23; rabbit collagen induced platelet aggregation and platelet adhesion are obviously inhibited; and local ischemic brain damage caused by formation of cerebral thrombosis is lessened by inhibiting the formation of cerebral thrombosis and ischemic brain tissues are obviously protected.
CN102846647A Veterinary drug for treating salmonellosis of fowl The invention discloses a veterinary drug for treating salmonellosis of fowl, and is characterized in that the veterinary drug comprises tylosin tartrate, ciprofloxacin hydrochloride and glucose. The inventive veterinary drug can effectively treat salmonellosis of fowl, has evident curative effect and is convenient to use, and can be widely popularized.
US20110230816 Gels for Transdermal Delivery The present disclosure provides hydrogels that are suitable for drug delivery. In embodiments, hydrogels of the present disclosure may be used for transdermal delivery of bioactive agents, including drugs. The hydrogels of the present disclosure may also be useful as conductive compositions for use with electrodes.
WO2012103113A1 Pyrazine and imidazolidine derivatives and their uses to treat hepatitis c Disclosed herein are compounds useful for treating a viral infection, such HCV.
CN1786003B Sulfur, nitrogen heterocyclic naphacyl imine cell compounds and its application in tumour cell The present invention relates to a sulfur-nitrogen heterocyclonaphthoylimine compound. It is obtained by adding heterocycle containing sulfur or/and nitrogen heteroatom on the arylcycle of naphthoylimine. Tests show that the invented compound has strong inhibitory effect for inhibiting in vitro tumor cell growth, and has high DNA hydrolysis activity.
WO2010029461A1 Heteroaryls amide derivatives and their use as glucokinase activators The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.
US7217555 isolated human NAALAD-ase (N-acetylated alpha-linked acidic dipeptidases) L protein; There is disclosed a cDNA molecule encoding human NAALAD-ases designated herein as L, II and IV and having the amino acid sequences illustrated in FIGS. 1, 3, 4 and 5. The NAALAD-ases themselves also form part of the invention. Further provided are expression vectors incorporating the cDNA molecules suitable for transforming a cell, tissue or organism.
EP1915156B1 Use of psychomotor stimulants and compositions containing them in a method of treating parturient placental mammals in order to reduce maternal and/or uterine exhaustion The present invention relates to a method of facilitating the birth process of placental mammals, especially to a method of reducing delays in the birth process and, thereby, complications resulting there from that may negatively affect the health and wellbeing of the mother and increase the incidence of stillbirths and/or neonatal mortality. According to the present invention delays in parturition that result from maternal and/or uterine exhaustion may be prevented or reduced by the administration of an effective amount of one or more psychomotor stimulants to the parturient mammal prior to and/or during parturition. Said psychomotor stimulant is selected from the group comprising xanthines and amphetamines.
US20100239522 Chemotherapeutic for inducing an msh2-dependent apoptotic pathway A method of treating cancer in a subject in need thereof comprises administering said subject reserpine, yohimbine, an analog thereof, or a pharmaceutically acceptable salt or prodrug thereof, in an amount effective to treat the cancer. Compounds and compositions useful for carrying out the method are also described.
CN103012314A Sulfonamide compound and preparation method as well as application thereof The invention discloses a sulfonamide compound and a preparation method as well as application thereof, and provides the sulfonamide compound with hypoglycemic activity and the preparation method thereof. The sulfonamide compound has a structure of a general formula I, wherein X is S or O atoms, n is 1, 2, 3 or 4, R1 and R2 are simultaneously or respectively hydrogen or C1-C4 alkyl groups, and R3, R4 and R5 are simultaneously or respectively one out of hydrogen, C1-C6 alkyl groups, C1-C4 alkoxyl groups, halogens, single or multi-halogen replaced C1-C4 alkyl groups, cyan, phenyl groups, single halogenated phenyl groups, C1-C4 alkoxyl phenyl group, C1-C4 alkyl sulfonyl groups and bromomethyl carbonyl groups. The sulfonamide compound with the structure of the formula I and pharmaceutically acceptable salts thereof have obvious effect in terms of resisting hyperglycemia.
EP2240471A1 Molecules comprising a bis(heteroaryl)maleimide backbone, and use thereof in the inhibition of dde/ddd enzymes The invention relates to molecules having a bis(heteroaryl)maleimide structure and exhibiting inhibitory characteristics with respect to enzymes which have a catalytic pocket comprising invariant D, D and E or D, D and D amino acids, such as transposases, RAG recombinases or retroviral integrases. The invention also relates to the use of these molecules for the in vitro, ex vivo or in vivo inhibition of transposases, of RAG recombinases and of retroviral integrases, such as the HIV virus integrase, and also the use of these molecules in the treatment of pathological conditions associated with these enzymes in an animal or human host, in particular in the treatment of AIDS.
CA2361605C Pyrimidine-2,4,6-triones as inhibitors of matrix metalloproteinases The novel compounds of formula (I) wherein R1 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substitued alkynyl, alkoxy, substituted alkoxy, aryloxy or alkylalkoxy, and R2 is aryloxy; pharmaceutically acceptable salts of an acidic compound of formula (I), and prodrugs thereof can be used in the treatment or control of cancer associated with overexpression of gelatinase-A and/or gelatinase-B, particularly skin cancer, breast cancer, prostate cancer, colon cancer, lung cancer, and gastric cancer, and are also useful for other diseases associated with unregulated degradation of extracellular matrix, including rheumatoid arthritis, osteoarthritis, multiple sclerosis, corneal ulceration, periodontal disease and the like.
WO2006090244A1 New adamantane derivatives as dipeptidyl, peptidase iv inhibitors, processes for their preparation, and pharmaceutical compositions containing them The present invention relates to dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula (A): wherein R1, R2, Y, and n are as defined herein, pharmaceutical compositions containing the same, processes for their preparation, and methods for treating disorders mediated by DPP-IV inhibition, such as diabetes, especially Type II diabetes, with them.
US7754250 Drugs comprising plant extracts used for prevention amyloid formation, deposition or accumulation; amyloid fibrils, amylin fibrils, or islet amyloid fibrils or pre-deposited amyloid fibrils in type II diabetes; amyloid inhibitor A method of treating an amyloid disease in a patient or inhibiting the formation, deposition, accumulation, or persistence, of amyloid fibrils, amylin fibrils, or islet amyloid fibrils, and/or dissolving or disrupting pre-formed or pre-deposited amyloid fibrils in type II diabetes in a mammalian subject. In the method a therapeutically effective amount of plant matter form the genus Uncaria, species Tomentosa is administered, preferably from the inner bark or root tissue of Uncaria Tomentosa.
CN200942187Y Selenium-enriched garlic piece The utility model discloses a selenium garlic flake, which comprises selenium garlic powder and a plurality layer of propolis layer coated outside the selenium garlic powder; the propolis layer is composed of propolis and food dye. The utility model can be taken conveniently and can control the taking dosage. Besides, as the selenium garlic powder is coated with a propolis layer and has good taste, it can be taken by patent allergic to spicy taste. The utility model can effect well after being taken two granules a day. The utility model has excellent effect for preventing and controlling cancer, stopping the development of AIDS and allergic disease, thus ensuring multiple health-improving benefits for human being.
US20100297091 Compositions and methods for treatment of melanomas In certain embodiments, an expression construct is provided that contains a tissue-specific promoter such as tyrosinase linked to one or more cytotoxin genes. The cytotoxin genes may be saporin genes. In certain embodiments, a vector is provided that contains an expression construct as discussed above. The vector may be an adeno-associated virus or an adenovirus. Further, neural stem cells may be provided that contain and/or produce a vector, which in turn contains an expression construct containing a tissue-specific promoter linked to one or more cytotoxin genes. In certain embodiments, methods of using the neural stem cells provided herein for production and delivery of an animal virus vector are provided. Methods for treating melanomas in a subject in need thereof are also provided by delivering an expression construct that contains a tissue-specific promoter linked to one or more cytotoxins. In certain embodiments, the melanoma is metastatic, and in certain embodiments the melanoma is a brain melanoma.
WO2013007167A1 Crystal form i of salt of dipeptidyl peptidase-iv inhibitor and preparation method and use thereof The present invention relates to the crystal form I of salt of dipeptidyl peptidase-IV inhibitor and the preparation method and use thereof. In particular, it relates to the crystal form I of dihydrochloride salt of compound (R)-2-[[7-(3-aminopiperidine-1-yl)-3,5-dimethyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridine-1-yl]methyl]benzonitrile of formula (1), which is a dipeptidyl peptidase-IV inhibitor, and the preparation method and use thereof. The features of the crystal form I of dihydrochloride salt of the dipeptidyl peptidase-IV inhibitor of formula (1) are characteristic peaks at 8.7±0.2°, 19.4士0.2°, 23.5±0.2°, 27.2±0.2° in X-ray powder diffraction indicated by an angle 2θ (°) using Cu-Kα radiation.
CN1813741A Medicinal composition containing amlodipine and terazosine The present invention relates to a medicine composition containing amlodipine and terazosin. Said invention contains one kind of medicinal dose amlodipine, amlodipine active metabolic product and amlodipine medicinal precursor or medicinal salt of amlodipine, amlodipine active metabolic product and amlodipine medicinal precursor, one kind of terazosin, terazosin active metabolic product and terazosin medicinal precursor or medicinal salt of terazosin, terazosin active metabolic product and terazosin medicinal precursor and medicinal carrier or excipient. Said medicine composition can be used for preventing and curing hypertension.
WO2011064753A1 Pharmaceutical compositions and therapeutic applications of a hydrocortisone derivative designated as deina The invention relates to the hydrocortisone derivative of formula (I), whose IUPAC name is 3-[3, 5-Dihydroxy-3-(2-hydroxy-acetyl)-3a, 6-dimethyl- 7-oxo-dodecahydro-cyclo- penta[alpha]naphthalen-6-yl] -propionic acid, designated as Deina®, for use in the treatment of atrophic tissues, particularly skin, cartilage, connective, and mucosal tissues and scalp skin.
US20050163839 Oral controlled release pharmaceutical composition containing metaxalone as active agent The present invention provides an oral controlled release pharmaceutical composition comprising metaxalone, a pharmaceutically acceptable release rate controlling excipient, and pharmaceutically acceptable excipients, wherein the oral controlled release pharmaceutical composition provides peak plasma levels at a time of about 3 hours or more after oral administration of the composition.
US6887459 Administering inhalant with particulate carrier or diluent for treatment of chronic obstructive pulmonary disease The use of a dry powder comprising (A) formoterol, or a pharmaceutically acceptable salt or solvate thereof, or solvate of said salt, and (B) a pharmaceutically acceptable particulate diluent or carrier in an amount of from 400 μg to 5000 μg per μg of (A) for the preparation of an inhalable medicament for the treatment of chronic obstructive pulmonary disease.
US20080214542 1-(5-methoxyisoindolin-2-yl)-6-[4-(3-trifluoromethylphenyl)piperazin-1-yl]hexan-1-one; amidation of an isoindole with a 4-phenylpyrimidinylalkanoic acid or amination of a N-haloalkylcarbonyl isoindole with a 4-phenylpyrimidine; antidepressant, neuroleptic agent; drug abuse, impotency, Parkinson's Disease The invention concerns compounds of general formula (I), a method for preparing same, as well as their use as therapeutic agent.
US20070254889 noninvasive technique for imaging and quantitating amyloid deposits; 2-phenyl- imidazo [1,2,a] pyridine derivatives; radiolabelling; drug delivery; 2-(4'-dimethylaminophenyl)-6-iodobenzothiazole The present invention is directed to pharmaceutical compositions comprising one or more compounds of Formulae I, II, III, IV, V, VI, VII, VIII, IX and X, or pharmaceutically acceptable salts thereof and excipients. The present invention provides a method of inhibiting β-amyloid plaque aggregation, the method comprising introducing into a mammal an aggregation-inhibiting amount of a compound of Formula I, II, III, IV, V, VI, VII, VIII, IX or X or a pharmaceutically acceptable salt, ester, amide or prodrug thereof. By inhibiting amyloid aggregation, this method is capable of rescuing cells that otherwise would be susceptible or further damaged by amyloidosis.
CN102100747B Method for preparing compound liquoric root tables The invention relates to a method for preparing compound liquoric root tables, which comprises the following steps of: sieving liquoric root extract powder and sodium benzoate with a 80-mesh sieve, and detecting whether foreign matters exist in appearance or not after sieving; mixing 14 kilograms of poppy capsule extract powder, 10 kilograms of talcpowder, 20 kilograms of liquoric root extract powder and 7 kilograms of sodium benzoate in a three-dimensional motion mixer of which the rotate speed of a motor is 800 revolutions/minute for 10 minutes to obtain a mixture A; mixing 51 kilograms of mixture A, 100 kilograms of liquoric root extract powder and 10 kilograms of talcpowder in the three-dimensional motion mixer of which the rotate speed of the motor is 800 revolutions/minute for 10 minutes to obtain a mixture B; mixing 161 kilograms of mixture B, 273.75 kilograms of liquoric root extract powder and 23.75 kilograms of talcpowder in the three-dimensional motion mixer of which the rotate speed of the motor is 600 revolutions/minute for 40 minutes to obtain a mixture C; dissolving 7 kilograms of star anise oil and 7 kilograms of camphor in 42.217 kilograms of 95 percent ethanol toprepare a bonding agent; and putting the mixture C in a spray drying pelletizer for 15 to 30 minutes, and spraying the bonding agent into a tank body under the pressure of 0.5 MPa, wherein the air inlet temperature is between 75 and 85 DEG C, and the yield is over 98 percent.
CN101721655A Repair oil for preventing and curing hand desquamate The invention relates to repair oil for preventing and curing hand desquamate, relating to a preparation of medicine. The repair oil is prepared by mixing the following components in parts by weight in a certain proportion: 10-12 parts of picked gentians, 8-10 parts of snake oil, 3-5 parts of fuligo e herbis, 23-25 parts of frankincense, 10-12 parts of radix curcumae, 6-8 parts of borneol, 3-5 parts of fructus cnidii and 13-15 parts of peppermint. The invention has exclusive prescription, can prevent and cure the recidivation of the hand desquamate, effectively kill the pathogenic bacteria, such as fungi, mycete, and the like, eliminate the scaled skin, contain and supplement nutrients for moistening and nourishing damaged skin and necessary for the repair process and achieve deep nourishing, surface nursing, prevention and nourishing combination and the effects of keeping palms without chapping and desquamating, repairing to be smooth and exquisite. The oil for is a Chinese materia medica preparation without side effect, has easy and convenient use and low cost and achieves the special effect through a large quantity of clinical tests.
WO2013037487A8 A particulate system for use in diminishing cell growth/inducing cell killing The Invention relates to a particulate system for use in diminishing cell growth, in particular the growth of cancer cells, comprising one or more water soluble lanthanide compounds that are embedded in a solid biodegradable polymer particle, the polymer being selected from the group consisting of polycarbonic acids, polylactic acids, polyglycolic acids, polypeptides or combinations thereof.
CN1923280A Anti-cancer slow release injection containing dichloroethylaminum Disclosed is an anticancer slow release injection containing diclothamin medicaments, wherein the constituents include anti-cancer drugs, slow release auxiliary materials, suspending agent and/or dissolvent. The anti-cancer drugs include leukeran, Cyclophosphamide, 4-hydroperoxycyclophosphamide, isoendoxan, the slow release auxiliary materials can be selected from polylactic acid, glycolic acid and glycolic acid copolymer, ethylene-vinylacetate copolymer or their combination, the suspending agent is selected from sodium carboxymethylcellulose or mannitol. The dissolvent is selected from distilled water, water for injection, physiological lotion, absolute ethyl alcohol, microcosmic salt or carbonates cushioning liquid. The anticancer slow release injection can be administered through subcutaneous, intracavity, intra-tumor, tumor-surrounding, intra- lymph gland or bone marrow channels, the whole body toxicity reaction of the anti-cancer medicament can be lowered, the tumor local medicinal concentration can also be selectively increased and maintained, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved.
CN101952294A Pyrrolopyrazine kinase inhibitors The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
CN103183634A 3-(2-isobutyl-5-(4-isobutylpiperidine-1-carbonyl)phenyl)propionic acid and preparation method thereof The invention provides a benzophenone analogue compound which has a structure as described in the specification. The compound has an excellent inhibitory effect on biological activity of protein AP-1.
WO2013146734A1 Anticancer agent The purpose of the present invention is to provide a novel anticancer agent effective against cancer. When an agent prepared using an extract of Arctium lappa seeds was injected into a pancreatic cancer patients such that the daily dose of arctigenin was 100mg or greater, a tumor shrinkage effect was observed and a decrease in tumor markers was confirmed. The present invention provides an anticancer agent containing arctigenin such that the daily dose is 100mg or greater. Further, the present invention provides an anticancer agent containing arctigenin and arctiin in a weight ratio arctigenin / arctiin = 0.7-1.3.
EP1867327A1 Astaxanthin and esters thereof for protecting neurocytes and treating Parkinson's disease A neurocyte protective agent that is capable of alleviating mitochondrial dysfunction and oxidative stress in neurocytes is provided. The neurocyte protective agent and the agent for protecting neurodegenerative diseases according to the present invention comprise astaxanthin and/or an ester thereof. In particular, the neurocyte protective agent of the present invention is effective in protecting against the degeneration of dopaminergic neurons of the substantia nigra and noradrenergic neurons of the locus ceruleus, and it is expected that ingestion of the neurocyte protective agent will serve as fundamental therapy for Parkinson's disease.
US6863693 Phospholipid-coated implants A prosthesis or implant has a surface carrying a coating comprising at least one phospholipid at a concentration to improve osteointegration. A method of making such a prosthesis or implant and a kit comprising a prosthesis or implant is also described.
CN103462941A Plaster for treating oral ulcer and preparation method of plaster The invention belongs to the technical field of biologic medicines, and relates to a plant polysaccharide plaster for treating oral ulcer and a preparation method of the plaster. The plaster is prepared from the formula with the following components in percentage by mass: 4-15% of bletilla striata polysaccharide, 0.1-0.4% of vitamin C, 0.0002-0.0005% of vitamin B12, 0.02-0.05% of vitamin E, 0.2-2% of glycerinum, 0.5-2% of tween-80 and the balance of distilled water, wherein vitamins refer to vitamin C, vitamin B12 and vitamin E, and the vitamins can not be added or one or two of the vitamins are added. The process comprises the following steps of crushing bletilla striata pieces, screening, extracting the bletilla striata polysaccharide by using a water extract and alcohol precipitate method, preparing a glue solution, filtering, degassing, cooling, forming a plaster, drying, dyestripping, shaping and packaging so as to obtain a finished product. The plaster has the characteristics that the use is convenient, the effect can be rapidly achieved, the curative effect is good, the plaster is safe and free of side effect, the price is low, and the like.
US20120295979 Use of sulindac for protecting retinal pigment epithelial cells against oxidative stress Compositions and methods described herein are based on the use of the drug sulindac, a non steroidal anti-inflammatory drug (NSAID), for protecting retinal pigment epithelial cells against oxidative stress which is a major component of macular degeneration. Described herein is a new use for sulindac.
US7476681 anticarcinogenic agent; prostate cancer, benign prostatic hyperplasia, prostatic intraepithelial neoplasia, hirsutism, acne, androgenic alopecia, or polycystic ovary syndrome, prostate, lung, pancreatic, colon, renal cancer, myeloid leukemia In its many embodiments, the present invention provides a novel class of compounds as illustrated below, wherein the various moieties are described herein, as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, pharmaceutical compositions containing one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17β-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.
CN1864667A A stable lyophilized preparation of rocuronium bromide and preparation method thereof The present invention relates to stable freeze dried rocuronium bromide preparation and its preparation process. The freeze dried rocuronium bromide preparation includes rocuronium bromide and freeze drying excipient in the weight ratio of 0.2-1. The freeze dried rocuronium bromide preparation needs no low temperature preservation and convenient storing, and is used for muscular relaxation of patient in surgical operation.
US20080226615 Vectors having both isoforms of beta-hexosaminidase and uses of the same Disclosed are compositions and methods related to delivering a nucleic acid to the central nervous system.
WO2013004141A1 3-alkoxy-substituted-2-pyrazinyl formamide compound and use thereof Disclosed are a 3-alkoxy-substituted-2-pyrazinyl formamide compound having a structure represented by formula I and use thereof in preparing anti-viral medications. The compound disclosed exerts anti-viral effects in vivo by means of metabolism into T1105 or T705 through esterate or P450 enzyme.
WO2011085291A1 1 - (2 - phenoxymethylphenyl) piperazine compounds as serotonin and norepinephrine reuptake inhibitors The invention relates to compounds of formula (I): where a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
US20080300226 Combination of Anticholinergics and Glucocorticoids for the Long-Term Treatment of Asthma and COPD The present invention describes the combination of topically inhaled medicinal formulations comprising an anticholinergic component and a glucocorticosteroid component and its use in the symptomatic and prophylactic treatment of diseases of the respiratory tract, especially with an obstructive component or underlying inflammation like asthma and chronic obstructive pulmonary disease (COPD). It further comprises the presentation of this combination in a locally applied (inhaled) formulation and application in an inhalation device for instance in the Novolizer®.
CN1935140A Compound diphenidol hydrochloride dispersible tablet, and its preparing method The present invention relates to a difenidol hydrochloride dispersion tablet preparation and its preparation method. Its composition includes (by wt%) 10%-50% of difenidol hydrochloride and 50%-90% of auxiliary material, in the auxiliary material the disintegrating agent content is 5%-20% of whole medicine component, said disintegrating agent can be one kind of cross-linked PVP, low-substituted hydroxypropyl cellulose and carboxymethyl starch sodium or their mixture. The auxiliary material also includes one kind of diluting agent, adhesive, corrective and flow aid or their mixture.
CN101434579A Fuziline esterification derivative, synthetic method and use The invention discloses a preparation method of a derivative (with a compound structure shown as the picture) of fuziline in a natural diterpenoid alkaloid of aconitum plants and an application thereof, pertaining to the technical field of medical and pesticide synthesis. The preparation method of the compound derivate comprises the steps that the fuziline is dissolved in a dry pyridine and subjected to alkaline treatment, chloroform extraction and steaming and concentration after being added with a sulfate reagent for a chemical reaction, thus obtaining the sulfated derivative; and a crude product can be purified by the method of recrystallization or column chromatography. The synthesizing method is simple and convenient and has relatively low cost and high transformation rate. The compound synthesized has relatively high biological activity and can be used for developing new products such as medicines, pesticides, etc. In the formula, R1 refers to alkanoyl, fatty acyl or aromaticacyl radical such as acetyl, propionyl, benzoyl, caproyl, p-chlorobenzene formyl, and the like; R2 refers to hydrogen atoms or alkanoyl, fatty acyl or aromaticacyl radical such as acetyl, propionyl, benzoyl, caproyl, p-chlorobenzene formyl, and the like; and R3 refers to hydrogen atoms or alkanoyl, fatty acyl or aromaticacyl radical such as acetyl, propionyl, benzoyl, caproyl, p-chlorobenzene formyl, and the like.
CA2216583C Levobupivacaine and its use as an anaesthetic in pregnant women Levobupivacaine is useful as an anaesthetic in pregnant women. For this or other purposes, it may be formulated in a relatively high concentration, e.g. above 0.75 %.
WO2010072354A1 MESYLATE SALT OF 5-(2-{[6-(2,2-DIFLUORO-2-PHENYLETHOXY)HEXYL]AMINO }-1-HYDROXYETHYL)-8-HYDROXYQUINOLIN-2(1H)-ONE AS AGONIST OF THE β2 ADRENERGIC RECEPTOR The present invention is directed to a mesylate salt of 5-(2-{[6-(2,2-difluoro-2- phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1 H)-one and pharmaceutically acceptable solvates thereof.
CN103156823A Ketoprofen controlled-release preparation and preparation method thereof The invention relates to a ketoprofen controlled-release preparation and a preparation method thereof. The preparation comprises a medicament-containing tablet core, a semi-permeable controlled-release coating membrane wrapping the tablet core and a medicament-containing rapid release layer outside the semi-permeable membrane. The medicament-containing tablet core comprises a main medicament, osmotic active substances, a filler and other pharmaceutical excipients; the semi-permeable controlled-release coating membrane comprises cellulose acetate, a pore forming agent and a plasticizer; and the rapid release layer comprises the main medicament and a water-soluble coating material. The invention further relates to the preparation method of the controlled-release preparation. The preparation is performed by adopting a conventional tablet preparation method, the preparation process is simple, and the main manifestation is that a single-layer osmotic pump tablet technology is applied to insoluble medicaments, the main medicament is suspended in the water-soluble coating material for preparing the rapid release layer, and the effective blood concentration of the medicament can be fast achieved. The medicament release of the preparation is in line with the zero-order release process, the medicament release is more complete, the administration frequency of patients can be effectively reduced, and the compliance of the patients can be improved.
US20120046320 Beta- and gamma-diketones and gamma-hydroxyketones as wnt/beta-catenin signaling pathway activators The present invention discloses β-diketones, γ-diketones or γ-hydroxyketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
WO2008125811A1 N-[HETEROARYLCARBONYL]-S-THIENYL-L-ALANINE DERIVATIVES AS α5β1 ANTAGONISTS The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to a5b1 antagonists that also exhibit appropriate selectivity profile(s) against other integrins.
WO2008035365A3 Rna interference mediated inhibition of aurorakinase b and its combinations as anticancer therapy This invention relates to the use of short nucleic acid molecules that modulate Aurora-B kinase (AurkB) expression. The invention includes compounds, compositions and methods useful for the modulation of expression and activity of genes involved in the AurkB pathway. In one embodiment, the present invention provides short nucleic acid molecules, such as siRNA, which can be used in treating, preventing, or inhibiting cancer, and any other proliferative disease, trait or condition, which respond to a reduction in AurkB expression in a cell or tissue. Such short nucleic acid molecules can be used alone or in combination with other treatments or therapies, including short nucleic acid molecules that modulate expression of EGFR.
CN103040781A Pramipexole dihydrochloride tablet composition and preparation method thereof The invention relates to a pramipexole dihydrochloride tablet composition and a preparation method thereof, in particular to a pramipexole dihydrochloride tablet which comprises the following materials in parts by weight: 0.1-2 parts of pramipexole, 200-500 parts of lactose and microcrystalline cellulose with the weight accounting for 10-90% of that of the lactose. The preparation method of the pramipexole tablet comprises the following steps that the materials pass through a 40-100-mesh sieve respectively, and are mixed uniformly and tabletted, therefore, the pramipexole dihydrochloride tablet is obtained. The pramipexole tablet obtained by the preparation method has an extremely excellent pharmacy property.
US20120172354 Substituted N-Phenyl-1-(4-Pyridinyl)-1H-Pyrazol-3-Amines The present invention relates to N-phenyl-1-(4-pyridinyl)-1H-pyrazol-3-amine derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to formula (I) Wherein R1, R2, R3, R4, R5, R6 have the meaning defined in the claims. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
US20090233976 Antimitotic Rhizoxin Deritivatives of Burkholderia Rhizoxina, Method for Producing Said Derivatives and Use Thereof The invention concerns four novel secondary metabolites of the Burkholderia rhizoxina endosymbiont, a method for isolating said compounds from cultures of the bacteria and the use of said substances. The invention aims at providing novel rhizoxin derivatives with an antimitotic effect. Therefore, the following substances 1-4 are isolated, said substances exhibiting potential antifungal, cytotoxic and antiproliferative properties.
US7910605 Administering tertiary amines, e.g., 3,3-Dimethylbutyl 3-piperidinopropyl ether, 3-Phenylpropyl 3-piperidinopropyl ether, or3-(4-Chlorophenyl)propyl 3-piperidinopropyl ether to treat cognitive disorders such as attention, wakefulness and memory disorders Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine.
CN101085351A Anticancer composition containing uramustine An anti-cancer composition comprises anti-cancer effective ingredient selected from tyrosine kinase inhibitor and/or uramustine and sustained release adjuvant, and can be made into sustained release injection and sustained release implant agent. Sustained release injection also comprises special dissolvent containing suspending agent. The Suspending agent has a viscocity of 100cp-3000cp (at 20deg.C-30deg.C) and is selected from sodium carboxymethylcellulose, and so on. the sustained release adjuvant is selected from p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP/TC), p(BHET-EOP/TC), p(BHDPT-EOP/TC), p( BHDPT-EOP/TC), p(CHDM-HOP) or p(CHDM-EOP).Slow releasing injection and implantable agent can keep high medicinal concentration in tumor part through slow releasing for over 60 days after being injected or implanted in or around tumour. The anticancer composition may also be prepared into sustained-release implant. It can reduce systemic toxic reaction of anticancer drugs, and also selectively improve the therapeutic effect of non-operative therapy such as chemotherapy.
CN103520153A Application of Eupalinolide K in preparing anticomplement drugs The invention discloses application of Eupalinolide K in preparing anticomplement drugs. The related research indicates that the Eupalinolide K has high anticomplement activity by complement classical pathway and bypass pathway and can be used for preparing anticomplement drugs.
EP2691394A1 Compounds for treatment of metabolic syndrome Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.
CN103565762A Blonanserin pharmaceutical composition with improved oral absorptivity A bonanserin pharmaceutical composition with improved oral absorptivity is characterized by comprising the components by weight: a first part: 4 g of bonanserin and 25 g of alpha cyclodextrin; and a second part: 20 g of cospovidone, 50 g of microcrystalline cellulose, 60 g of lactose, 20 g of pregelatinized starch, 1 g of powdered steatile, 1 g of magnesium stearate and proper amount of a povidone anhydrous-alcohol solution with a ratio of 5%.
US20110287110 Combination cancer treatment Described herein are methods of inhibiting the proliferation of cancer cells and methods of treating cancer, by administering a combination of a copper chelator and a platinum-based chemotherapeutic.
EP0882134B1 Methods and compositions for protective and therapeutic genetic immunization Disclosed and claimed are methods and compositions for raising protective and therapeutic immunity in humans and animals by genetic immunization. The subject invention combines both safety and efficacy in the treatment of viral infections and diseases caused thereby. The methods of the subject invention comprise transduction of cells with a construct that directs the expression of an attenuated virus not capable of causing disease, for example, replication-incompetent. The enhanced efficiency of the subject invention in generating an antiviral immune response is due in part to a unique method for vehiculating attenuated viral particles within the host human or animal. Specifically, the attenuated non-pathogenic viral particles of the subject invention which produce the therapeutic or preventative immune response are generated by cells in the lymphoid organs such that the release of the viral particles occurs in the location within the human or animal body where antiviral responses are generated by cells of the immune system. The release of the virus particles in the lymphoid organs is achieved by transducing host cells of the lymphoid organs (or cells which migrate preferentially to the lymphoid organs) with a genetic construct which results in expression of the attenuated virus. As described more fully herein, transduction of dendritic cells is particularly preferred.
US20120308658 Methods and compositions to treat hemorrhagic conditions of the brain The described invention provides a nonhuman animal model system for hemorrhagic brain conditions, methods for evaluating a substance for treating the hemorrhagic brain condition in a mammal, methods for treating hematoma expansion or recurrent rebleeding resulting from hemorrhagic brain conditions in a mammal, and pharmaceutical compositions for administration into or at a distance proximal to the hemorrhagic brain condition.
WO2008132846A1 Tricyclic heteroaryl compound Disclosed is a compound which has a squalene synthase inhibition activity and a cholesterol synthase inhibition activity and is useful as a medicinal agent such as a prophylactic and/or therapeutic agent for hyperlipemia (including hypercholesterolemia, hypertriglyceridemia and hypo-HDL-cholesterolemia) and/or arteriosclerosis in a mammal including human. Specifically disclosed is a specific compound such as (1) 2-[(4R,6S)-8-chloro-6-(2-chloro-3-ethoxyphenyl)-1-(trifluoromethyl)-4H,6H-[1,2,4]triazolo[4,3-a][4,1]benzoxazepin-4- yl]acetic acid and (2) 2-(1-[2-[(4R,6S)-8-chloro- 6-(2-chloro-3-ethoxyphenyl)-1-(trifluoromethyl)-4H,6H- [1,2,4]triazolo[4,3-a][4,1]benzoxazepin-4-yl]acetyl]-4- piperidinyl)acetic acid.
WO2008003511A1 Use of aminothiazole derivative compounds, pharmaceutical compositions thereof, in the treatment of diseases characterized by abnormal repression of gene transcription, particularly huntington's disease The present invention relates to the use of aminothiazole compounds and pharmaceutical compositions thereof in the medical practice. More specifically, the instant invention relates to the use of aminothiazole derivatives and pharmaceutical compositions thereof in the treatment and/or prophylaxis and/or prevention of diseases and/or pathological conditions characterized by the abnormal repression of gene transcription and/or by neurodegeneration, particularly the Huntington's disease.
EP1799215A2 Chemokine-binding heterocyclic compound salts, and methods of use thereof The present invention relates to chemokine-binding heterocyclic compound salts, methods of use thereof, and methods for preparing the same.
DE202006000591U1 Composition useful for providing nutrients to healthy joints, comprises glucosamine, chondroitin, copper salt, selenium salt in rapid-release form and vitamins C, E, B6 and B12, folic acid, zinc salt, manganese salt in delayed-release form Combined dry preparation (A) comprises (a) glucosamine, chondroitin, at least one copper salt and at least one selenium salt in a form providing quick release in the digestive tract and (b) vitamins C, E, B6 and B12, folic acid, at least one zinc salt and at least one manganese salt for delayed release in the digestive tract.
EP1833812A1 N-[(4, 5-diphenyl-3-alkyl-2-thienyl) methyl]amine (amide, sulfonamide, carbamate and urea) derivatives as cannabinoid cb1 receptor antagonists The invention concerns compounds of formula (I), wherein: X represents a -C-, -SO2-, -C-N(R6)-, -C-O- group; R1 represents a (C1-C7)alkyl, a (C3-C7)cycloalkylmethyl unsubstituted or substituted several times on the carbocycle, an unsubstituted of mono-, di- or trisubstituted phenyl; an unsubstituted or mono-or disubstituted benzyl, an indolyl; R2 represents a hydrogen atom or a (C1-C3)alkyl; R3 represents a (C1-C5)alkyl or a (C3-C7)cycloalkyl; R4 represents an unsubstituted or mono-, di- or trisubstituted phenyl; R5 represents an unsubstituted or mono-, di- or trisubstituted phenyl; R6 represents a hydrogen atom or a (C1-C3)alkyl. The invention also concerns a method for preparing said compounds and their use as cannabinoid CB1 receptor antagonists.
CN103230362A In-situ gel for injecting flunixin meglumine and preparation method thereof The invention belongs to the field of a special pharmaceutical preparation for animals, and relates to an in-situ gel preparation for injecting flunixin meglumine and a preparation method thereof. The in-situ gel preparation is prepared from water as a solvent, flunixin meglumine, in-situ gel matrix known in the field, and other pharmaceutical necessary auxiliary materials. The preparation method is clarified. The preparation disclosed by the invention is liquid which freely flows at room temperature; sold or semi-solid gel is formed after dosing by intramuscular injection or subcutaneous injection; drug release is delayed; the lasting time is long; just one-time dosing in a course of treatment is achieved; and the in-situ gel has the advantages that the in-situ gel is simple to prepare, stable in property, convenient to dose, strong in animal adaption, and the like. The preparation disclosed by the invention has the effects of relieving fever, easing pain, diminishing inflammation and the like, and is used for preventing and treating diseases of animals such as pigs, sheep, dogs, cats, cattle and birds.
CN1730475A Aromatic amine ketene compounds, its synthesis method, pharmaceutical composition containing same and uses The invention provides arylamine alkenone compounds having a general formula (I), the preparation of the compounds, the medicinal composition containing them and the use of these compounds in preventing and/or treating platelet activating factor related diseases, especially the use in antiphlogistic immunization, in particular for treating acute or chronic inflammation, such as osteoarthritis, chronic infectious arthritis etc.
EP0986408B1 New medicaments based on polymers composed of methacrylamide-modified gelatin The present invention relates to a medicament comprising a biopolymer matrix comprising cross-linked vinyl-derivatives of gelatin, or co-polymerized methacrylamide modified gelatin with vinyl-modified polysaccharides, or cross-linked vinyl-substituted polysaccharide and gelatin being physically entrapped in a semi-interpenetrating network. Preferably said polysaccharide comprises dextran or xanthan. The present invention relates to a wound dressing or a controlled release device comprising said biopolymer matrix. Preferably said matrix is in the form of a hydrated film, a hydrated or dry foam, dry fibres which may be fabricated into a woven or non-woven tissue, hydrated or dry microbeads, dry powder, or covered with a semipermeable film, so as to control the humidity of the wound covered with the dressing, with the permeability chosen so as to maintain this humidity within a therapeutically optimal window.
CN101444603B Pharmaceutical composition for slimming and preparation method thereof The invention discloses a pharmaceutical composition for slimming and a preparation method thereof. The bulk drugs comprise ginseng, hairy antler, sesame, ganoderma lucidum, mays, boxthorn, black kerneled rice, Chinese date, fruit of hawthorn, maize, barley, salt and vitamin B. The pharmaceutical composition can be prepared into does types which can be accepted clinically by adding pharmaceutically conventional auxiliary materials according to the conventional process. The pharmaceutical composition has the functions of appeasing sustenance, promoting the production of body fluid to quench thirst, avoiding partial food, reducing fat, reducing weight and beautifying body, slimming and beauty treatment, reducing blood fat, reducing blood sugar, regulating viscera, supporting the healthy energy and prolonging life, and has obvious treatment effects on adiposity, diabetes, fatty liver and other diseases.
CN1686145B Doxycycline oral cavity adhesion tablet An adhesive oral tablet of doxycycline for treating periodontitis by adhering it onto suffered position is proportionally prepared from doxycycline or its salts or its hydrates, water-soluble polymer as adhesive matrix and additive.
US20130046009 Rho kinase inhibitors for treatment of mastocytosis and acute myeloid leukemia The disclosure is directed to methods of treating hematologic malignancies. More particularly, the disclosure is directed to methods of treating hematologic malignancies using Rho kinase (ROCK) inhibitors and myosin light chain-specific inhibitory RNA molecules. The disclosure is further directed to methods of identifying drug candidates for inhibiting ROCK in hematologic malignancies.
US20110183935 Heartwater There is provided a water product for general consumer comprising water suitable for human consumption and a food additive in the amount effective to alter a level of serum marker that indicates a likelihood of cardiovascular disease, thereby the water product is intended to lower the risk of cardiovascular disease of said general consumer. The preferred additive is Barliv™ betafiber.
US20100209495 Granulates, process for preparing them and pharmaceutical products containing them A granulate for use in a pharmaceutical composition and a pharmaceutical composition manufacture using the granulate, where the granule comprises an active pharmaceutical ingredient (API) having a poor water solubility (i.e., less than about 1 mg/mL) which is intimately associated with at least one pharmaceutically acceptable hydrophilic polymer. The granule optionally contains one or more pharmaceutically acceptable excipients, such as disintegrants, wetting agents, diluents, binders, lubricants, glidants, coloring agents and flavoring agents. The invention also relates to a process for preparing the pharmaceutical granulate and pharmaceutical compositions containing the granulate.
US20110196032 Pharmaceutical Dosage Form of an Antidepressant The present invention relates to pharmaceutical dosage forms of an antidepressant. More particularly, the present invention relates to pharmaceutical dosage forms of Escitalopram oxalate. The present invention also relates to a process for the preparation of pharmaceutical dosage forms of Escitalopram oxalate.
CN1927224A Emulsion for treating skin inflammation Disclosed is an emulsion for treating skin inflammations, wherein the main constituents include calamine, zinc oxide, glycerin, suspension auxiliary agent AC, Tween-60 and distilled water.
US20080139455 (2S,3S,E)-2-amino-14,14-difluoro-3-hydroxytetradec-6-enoic acid; serine palmitoyl transferase ; insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia Novel compounds, compositions comprising compounds, and methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, restenosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyltransferase activity.
CN101392015A Triterpene saponin in camellia seeds, preparation method and medical use thereof The invention pertains to the field of medical technology and provides triterpenoid saponin in camellia seeds, and a preparation method and medical application thereof. The triterpenoid saponin is shown in a general formula (1), wherein, R1 is hydrogen or oxhydryl or acyloxy; R2 is the hydrogen or the acyloxy; R3 is the hydrogen or the acyloxy; R4 is the hydrogen or the acyloxy; R5 is methyl or methylol or aldehyde group or carboxyl or metheyl carboxyl; R6 is the hydrogen or orglycosyl; the preparation method comprises the following steps: macroporous resins are degreased, extracted by ethanol, decocted in water, desugared and decolored to obtain crude total saponins and then go though an opened ODS chromatographic column and repeated HPLC method to obtain the total saponins of camellia seeds and monomer theasaponin. The triterpenoid saponin compounds in the camellia seeds have the functions of protecting gastric mucosa, being antineoplastic, reducing blood sugar and blood fat and thelike and are used for preparing medicaments or health-care foods having the functions of protecting gastric mucosa, being antineoplastic and reducing blood sugar and blood fat.
CN103446170A SGLT2 (Sodium-glucose co-transporter 2) inhibitor and use thereof The invention relates to the field of medicinal chemistry, and particularly relates to compounds (1-25) and a medicinal use of a medicinal composition containing the compounds, in particular a use as an SGLT2 (Sodium-glucose co-transporter 2) inhibitor.
US7667040 Azacyclic ethynyl derivatives Azacyclic ethynyl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
WO2006082400A1 Indan-amide derivatives with glycogen phosphorylase inhibitory activity A compound of the formula (1) or a pharmaceutically-acceptable salt: (A chemical formula should be inserted here - please see paper copy enclosed herewith) (1) possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
US7008765 polynucleotides that code for prostate specific antigen proteins or polypeptides; cells containing the recombinant nucleic acid molecules; hybridomas containing the antibodies; kits containing probes or antibodies; prevention of prostate cancer The present invention relates, in general, to a prostate-specific antigen, PCA3. In particular, the present invention relates to nucleic acid molecules coding for the PCA3 protein; purified PCA3 proteins and polypeptides; recombinant nucleic acid molecules; cells containing the recombinant nucleic acid molecules; antibodies having binding affinity specifically to PCA3 proteins and polypeptides; hybridomas containing the antibodies; nucleic acid probes for the detection of nucleic acids encoding PCA3 proteins; a method of detecting nucleic acids encoding PCA3 proteins or polypeptides in a sample; kits containing nucleic acid probes or antibodies; bioassays using the nucleic acid sequence, protein or antibodies of this invention to diagnose, assess, or prognose a mammal afflicted with prostate cancer; therapeutic uses; and methods of preventing prostate cancer in an animal.
EP1382336B1 Use of the abc expression promotor pioglitazone for the treatment of arteriosclerosis obliterans ABC-A1 mRNA expression promoters, LXRα mRNA expression promoters, ABC-G1 mRNA expression promoters, cholesterol transport promoters and cholesteryl ester accumulation inhibitors containing PPARδ modulators such as pioglitazone; ABC-G1 mRNA expression promoters containing PPARδ modulators; or ACAT-1 mRNA expression promoters and CEH mRNA expression promoters containing PPARδ modulators such as pioglitazone. These agents are excellent in the ability to control cholesterol distribution in vivo and have low toxicity.
CA2726987C Stat3 inhibitors Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.
WO2013130358A1 Macrocyclic compounds This invention relates to novel macrocyclic compounds (e.g., those delineated in the formulae herein), pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the protease elastase.
US20110212972 Compositions and Methods for Treating Female Sexual Dysfunction This invention relates to methods, pharmaceutical compositions and kits useful in treating female sexual dysfunction and the use of an estrogen agonist/antagonist for the manufacture of a medicament for the treatment of female sexual dysfunction. The compositions are comprised of an estrogen agonist/antagonist as a first active ingredient and a cyclic guanosine 3′,5′-monophosphate elevator as a second active component and a pharmaceutically acceptable vehicle, carrier or diluent. The compositions and methods of treatment are effective while substantially reducing the concomitant liability of adverse effects associated with estrogen administration.
US20100081694 Composition comprising at least one ppar agonist and a lipid component The present invention relates to compositions comprising at least one peroxisome proliferator-activated receptor (PPAR) agonist and a lipid component and to pharmaceutical ingredients comprising said ingredients. Such compositions are particularly suitable for the prophylaxis and/or the treatment of diseases such as diabetes, obesity and hypertriglyceridemia.
WO2010015585A1 6-benzyl-2,3,4,7-tetrahydro-indolo[2,3-c]quinoline compounds The present invention pertains to 6-benzyl-2,3,4,7-tetrahydro-indolo[2,3-c]quinoline compounds of formula (I), as well as the resulting pharmaceutical compositions, and their use in the treatment or prophylaxis of diseases alleviated by inhibition of type 5 phosphodiesterases. Furthermore, the present invention pertains to the methods of manufacturing these 6-benzyl-2,3,4,7-tetrahydro-indolo[2,3-c]quinoline compounds.
WO2008051862A2 Immunopotentiating compositions comprising beta-1,3/1,6-d-glucan and uses thereof The present invention provides compositions comprising beta-1,3/1,6-D-glucan and an additive (e.g.,, Vitamin D, Zinc, etc.) and methods of use, e.g., enhancing the immunocompetence of animals, e.g., humans, comprising administering the compositions of the invention to the animals.
US20120129803 Composition containing chitooligosaccharide for recovering from fatigue Disclosed is an anti-fatigue composition containing chitooligosaccharide as an active ingredient. The composition exhibits a fatigue recovery effect, and thus can be widely used in the health food or medical field.
EP2736491A2 Bepotastine compositions Novel compositions including bepotastine besilate and a corticosteroid are provided, compositions including at least about 0.008% w/v benzalkonium chloride, and compositions including hydroxypropylmethyl cellulose E15 LV.
CN102579426A Application of parthenolide as platelet-activating factor (PAF) antagonist The invention discloses application of parthenolide as a platelet-activating factor (PAF) inhibitor. The parthenolide can be used as a safe PAF antagonist to be applied to treatment, auxiliary treatment and prevention of diseases such as thrombus, atherosclerosis, ischemic cardio-vascular disease, cerebral ischemia, acute pancreatitis, endotoxic shock, asthma, hepatic fibrosis and hepatocirrhosis, injury of nerve, gastrointestinal ulcer and necrosis, psoriasis, systemic lupus erythematosus and acquired immune deficiency syndrome related to platelet-activating factor.
WO2005014597A1 N-[3-(3-SUBSTITUTED-PYRAZOLO[1,5-a]PYRIMIDIN-7-YL)PHENYL]-SULFONAMIDES, AND COMPOSITIONS, AND METHODS RELATED THERETO The present invention relates to compounds of Formula (I): wherein R1, R2 and R3 are as defined in the claims. The compounds have specific affinity for the GABAA receptor and are therefore useful in the treatment and prevention of diseases modulated by the α1- and α2-GABAA receptors.
CA2729684A1 Compositions and methods for promoting vascular barrier function and treating pulmonary fibrosis Active agents and compositions that promote barrier function or that inhibit permeability of the vascular endothelium associated with pulmonary inflammation are described.
CA2658911A1 Pyrimidine compounds for combating pathogenic fungi and cancer The present invention relates to the use of pyrimidine compounds of formula (I), wherein the variables have the meaning stated in the claims and in the description, for combating pathogenic fungi, new pyrimidine compounds of formula (I), and fungicides and pharmaceutical agents containing the same.
US20090023805 Method of administration The present invention relates to the use of mycophenolic acid, a salt or prodrug thereof in immunosuppression, particularly for prevention or treatment of transplant rejection and immune-mediated and/or inflammatory diseases, wherein mycophenolic acid, the salt or the prodrug thereof is administered with an initial intensified dosage regimen.
CA2446939C Pyridylpyrimidine derivatives as effective compounds against prion diseases The present invention relates to pyridylpyrimidine derivatives of the general formula (I) : wherein R represents hydrogen or methyl and Z represents nitrogen containing functional groups, the use of the pyridylpyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of prion infections and prion diseases, as well as compositions containing at least one pyridylpyrimidine derivative and/or pharmaceutically acceptable salt thereof. Furthermore, the present invention is directed to methods for preventing and/or treating prion infections and prion diseases using said pyridylpyrimidine derivatives. Human cellular protein kinases, phosphatases and cellular signal transduction molecules are disclosed as targets for detecting, preventing and/or treating prion infections and diseases, especially BSE, vCJD, or CJD, which can be inhibited by the inventive pyridylpyrimidine derivatives.
CN1582932A Hydroxycamptothecin liposome and its preparation A hydroxy camptothecin lipid used for preparing freeze-dried powder injection is prepared from hydroxy camptothecin, phosphatide or cholesterine through dissolving them in organic solvent, spinning evaporating at 40-70 deg.C to become film, adding the buffering liquid containing surfactant, cold storing for hydrating, and stirring.
US20120040887 Composition for the treatment of osteomyelitis, method for preparing the same, and method for the treatment of osteomyelitis The disclosure provides a composition for the treatment of osteomyelitis and a method for preparing the same. The composition includes: 100 parts by weight of water; 0.06-0.1 parts by weight of an antibiotic; and 5-40 parts by weight of a biodegradable thermosensitive polymer, wherein the biodegradable thermosensitive polymer has a structure as following: wherein, R1 is hydrogen, or —C(═O)—R2; R2 is C7-30 alkyl substituted or unsubstituted with functional groups; R3 is hydrogen, or C1-6 alkyl; and x, y or z individually are integers greater than 0.
US7713569 Therapeutic and anti-oxidant for variety of health purposes, including treatment of skin damage; also useful as a natural antibacterial, antiviral and fungicidal agricultural product The invention provides olive-derived hydroxytyrosol. According to one aspect of the invention, vegetation water is collected from olives. Acid is added to stabilize the vegetation water and prevent fermentation. The mixture is incubated to allow oleuropein to convert to hydroxytyrosol, and then fractionated to separate hydroxytyrosol from other components. The hydroxytyrosol is useful as a therapeutic and anti-oxidant for a variety of health purposes, including for the treatment of skin damage. In addition, the hydroxytyrosol is useful as a natural anti-bacterial, anti-viral and fungicidal product for agricultural and pest control applications.
US20110172234 Methods and compositions of trail-death receptor agonists/activators This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies.
US7977468 Chromosome 3p21.3 genes are tumor suppressors Tumor suppressor genes play a major role in the pathogenesis of human lung cancer and other cancers. Cytogenetic and allelotyping studies of fresh tumor and tumor-derived cell lines showed that cytogenetic changes and allele loss on the short arm of chromosome 3 (3p) are most frequently involved in about 90% of small cell lung cancers and greater than 50% of non-small cell lung cancers. A group of recessive oncogenes, Fus1, 101F6, Gene 21 (NPRL2), Gene 26 (CACNA2D2), Luca 1 (HYAL1), Luca 2 (HYAL2), PL6, 123F2 (RaSSFI), SEM A3 and Beta* (BLU), as defined by homozygous deletions in lung cancers, have been located and isolated at 3p21.3.
WO2013170186A1 Carbazole-containing sulfonamides as cryptochrome modulators The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing' s syndrome, and glaucoma.
US20120269881 Transdermal drug delivery device including an occlusive backing A transdermal drug delivery system for the topical application of one or more active agents contained in one or more polymeric and/or adhesive carrier layers, proximate to a non-drug containing polymeric backing layer which can control the delivery rate and profile of the transdermal drug delivery system by adjusting the moisture vapor transmission rate of the polymeric backing layer.
CN102018965A Application of miRNA-10a in preparation of drug inhabiting intrusion and transfer of colorectal cancer The invention discloses an application of miRNA-10a in the preparation of a drug inhabiting intrusion and transfer of colorectal cancer, and the miRNA-10a is a nucleotide sequence shown as SEQ ID NO.1 in a sequence table. The experiment reveals that compared with the miRNA-10a exoressed in a low transitivity cell strain SW480, the miRNA-10a is expressed at low level in the high transitivity cell strain SW620; Northern bolt and real-time quantitive PCR(polyperaze chain reaction) experiment also prove that the miRNA-10a is expressed at low level in a high transitivity colorectal cancer cell strain and clinical specimen; cell miRNA-10a level of SW620 can be improved through transfecting pri-miR-10a, so that the instrusion activity of the cancer cell is lowered obviously, and similar results also can be seen in the other high transitivity colorectal cancer cell strains. The experimental result reveals that the miRNA-10a inhabits the intrusion of the colorectal cancer cell in vitro, and the transfer of the colorectal cancer cell in vivo.
WO2010074586A1 Pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine derivatives and their use in cancer therapy The invention relates to pyrazolo[1,5-a]pyridine and/or -imidazo[1,2-a]pyridine derivatives, to their preparation, to their use as agents or drugs for cancer prevention or therapy for treating cancer, either alone or in combination with radiation and/or anticancer drugs.
US20050038069 Tumor necrosis factor antagonist; antiinflammatory agents; such as 2-Cyclopropyl-4-(3,5-dimethyl-4-pyridylmethoxy)-7-methoxy-3H-benzimidazole This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z1 represents a direct bond R1 may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R2 represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, hydroxy, —SO2NR4R5, —NR4SO2R5, —NR4R5, —C(═O)R5, —C(═O)C(═O)R5, —C(═O)NR4R5, —C(═O)OR5, —O(C═O)NR4R5, or —NR4C(═O)R5; R3 represents —C(=Z)—N(R7)R6, —C(=Z)—CHR12R6, —C(=Z)—R6, —CR8═C(R9)(CH2)p—R6, —C(R10)═C(R11)R12, —C(R13)(R10)C(R11)(R 14)R12, —C(R8)(R15)CH(R9)(CH2)p—R6, —R6, —N(R16)C(=Z)R6, —C(R17)═N—OC(=0)R18, —C(═O)—N(R19)OR20, —C≡C—R6, —CH2—C(=Z)—R6, —C(=Z)—C(=Z)R6, —CH2—NHR6, —CH2-ZR6, —CH2—SOR6, —CH2—SO2R6, —CF2—OR6, —NH—CH2R6, -Z-CH2R6, —SO—CH2R6, —SO2—CH2R6, —O—CF2R6, —O—C(=Z)R6, —N═N—R6, —NH—SO2R6, —SO2—NR21R22, —CZ-CZ-NHR6, —NH—CO—OR6, —O—CO—NHR6, —NH—CO—NHR6, —R23, —CX1═CX2R6, —C(═NOR24), —(CH2)qR6, —CH2—CO—NH(CH2)qR6, —CH2—NH—CO(CH2)qR6, —CH2—CO—CH2R6, —C(═NR25)—NH(CH2)qR6, —C(X3)═N—(CH2)qR6 or —CH(X4)—CH2R6; A1 represents a direct bond, or a straight or branched C1-6 alkylene chain optionally substituted by hydroxyl, alkoxy, oxo, cycloalkyl, aryl or heteroaryl, or A1 represents a straight or branched C2-6alkenylene or C2-6alkynylene chain; Z1 represents a direct bond, an oxygen or sulphur atom or NH; n and m each represent zero or 1, provided that n is 1 when m is zero and n is zero when m is 1; and N-oxides thereof, and their prodrugs, and pharmaceutically acceptable salts and solvates of the compounds of formula (I) and N-oxides thereof, and their prodrugs. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.
CA2338896C Fast dissolving ibuprofen containing compositions having analgesic activity An analgesic composition useful in the preparation of fast dissolving tablets is provided wherein the composition is the result of combining ibuprofen, arginine, linear PVP and an alkaline bicarbonate to which usual excipients for the preparation of tablet are added.
US7144710 Method for detecting inflammation and inflammatory conditions Methods for detecting the inflammatory biomarkers molecule CD 163 in biological samples are provided. Also provided are methods for monitoring the course of an inflammatory process or condition in a patient and compositions and methods for preventing and treating inflammation and inflammatory processes.
CN103405390A Preparation method of lecithin-bound iodine enteric-coated pellet tablet The invention discloses a preparation method of a lecithin-bound iodine enteric-coated pellet tablet. The preparation method comprises the following steps: uniformly mixing lecithin-bound iodine with auxiliary materials, wherein the auxiliary materials include one or more of a disintegrating agent, an excipient and a diluent; adhering the mixed auxiliary materials onto the surface of a starch or lactose pellet to obtain pellet particles by an adhesive in a ratio of the adhesive to the auxiliary materials of (0.05-0.5) to 1; adding the pellet particles into the auxiliary materials after being wrapped with enteric coatings and then directly tabletting, or mixing the pellet particles with buffer particles which are prepared by a conventional method in a weight ratio of (1:1) to (2:8) to obtain the pellet tablet. Compared with the conventional preparation, the pellet tablet, which is prepared by the preparation method disclosed by the invention, has the characteristic that the distribution area is large, and has the advantages of being small in size, capable of dividing dosage and the like, so that patient compliance is increased; the pellet can be isolated from the air more stably, and a period of validity reaches three years or more,.
US20110190366 Substituted 2-indolinone as ptk inhibitors containing a zinc binding moiety The present invention relates to substituted 2-indolinone containing zinc-binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
WO2014086790A1 Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a (I) The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.
CN103193851A Steroidal diene amide compound as well as preparation method and application thereof The invention belongs to the field of pharmaceutical chemistry and relates to a steroidal diene amide compound as well as a preparation method and an application thereof. The compound is as shown in a formula I, and in-vitro anti-tumor activity experiments prove that the compound has broad-spectrum anti-tumor activity and has good inhibition action against a variety of human cancer cells, such as EC109, MGC-803, MCF-7, PC-3 and SMMC- 7721; and the compound is suitable for researching anti-tumor lead compounds or preparing novel anti-tumor medicaments. The synthesis method is simple, convenient and suitable for industrial production.
CN101032507B Bacteria resisting medicine of erythrocin nanometer-emulsion and the preparing method The nanometer antibacterial erythromycin medicine consists of erythromycin in 0.5-1.5 wt% and nanometer emulsion matrix in 98.5-99.5 wt%. It is yellowish transparent liquid, and has medicine granularity of 1-100 nm, low viscosity, high stability, fast absorption, targeted medicine release, high bioavailability, less toxic side effect and other features. The medicine may be attached well onto bacteria and permeated into bacteria to disturb their metabolism and to reach bacteriostasis and bactericidal effect. It is used mainly for treating serious infection caused by penicillin resisting staphylococcus aureus and hemolytic streptococcus as well as chicken's chronic respiratory tract disease, malignant rhinitis, etc. The medicine has simple preparation process, less toxicity and high safety.
WO2009013846A1 Pharmaceutical composition for amelioration of lower urinary tract symptom associated with prostatomegaly Disclosed is a pharmaceutical composition comprising (R)-5-(2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl)-2-methoxybenzene-1-sulfonamide (tamsulosin) or a pharmaceutically acceptable salt thereof and (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate (3R)-quinuclidin-3-yl ester (solifenacin) or a pharmaceutically acceptable salt thereof as active ingredients, particularly a pharmaceutical composition for ameliorating a lower urinary tract symptom associated with prostatomegaly. Also disclosed is use of a combination of tamsulosin or a pharmaceutically acceptable salt thereof and solifenacin or a pharmaceutically acceptable salt thereof for the amelioration of a lower urinary tract symptom associated with prostatomegaly. Further disclosed is a combination therapy.
EP2311472A1 Cognitive disorder-ameliorating agent A cognitive impairment ameliorant is provided that is useful for the prevention or treatment of cognitive impairment, and particularly Alzheimer's disease. The cognitive impairment ameliorant contains royal jelly as an active ingredient thereof.
WO2006020156A2 Heterocyclic dye compounds for in vivo imaging and diagnosis of alzheimer’s disease The present invention relates to the identification of compounds that are suitable for imaging amyloid deposits in living patients. The invention relates, in part, to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease. The present invention also relates to therapeutic uses for such compounds, as examplified by compounds of the formula (I) in which Y is independently S, O, or N and m is 1, 2, or 3.
CN101406482A Composition for preventing and treating crustacean disease The invention relates to the field of preventing and treating diseases of aquaculture animals, in particular to a composition for preventing and treating crustacean diseases for crustaceans. The composition comprises the following components in weight portion: 5 to 15 portions of vitamin D3, 3 to 9 portions of vitamin, 15 to 30 portions of calcium dihydrogen phosphate, 0.1 to 0.6 portions of citric acid, and 46 to 47 portions of vector. The composition has the advantages of having growing and recovering functions for carapaces of crustaceans and the hardness after exuviation, improving the survival rate of exuviation, increasing the bright color and the gloss of the body surfaces of the crustaceans, assisting the treatment of crustacean ulcer, improving the disease resistant and anti-stress capabilities, and increasing the hardness of the carapaces to improve the yield.
US6858628 Substituted cyclic amine metalloprotease inhibitors The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
US7026270 malayamycin A and desmethylmalayamycin A prepared from a previously unknown strain of Streptomyces malaysiensis, used for combating or controlling phytopathogenic fungi This invention concerns new biocidal compounds of formula (I) wherein R is H or CH3. Of particular interest are two isomers that are named malayamycin A and desmethylmalayamycin A. These isomers, which may be prepared by growing under controlled conditions a previously unknown strain of micro-organism from the species Streptomyces malaysiensis, are characterised by nmr and mass spectroscopic data. They have biocidal activity, including anti-fungal, anti-viral and anti-cancer activity, and are of special interest for use in agriculture, horticulture, animal and human health.
US20080299190 Direct Compression Formulation and Process This invention relates to tablets especially tablets formed by direct compression of a dipeptidylpeptidase IV (DPP-IV) inhibitor compound, a process for the preparation thereof; to new pharmaceutical formulations, and new tableting powders comprising DPP-IV inhibitor formulations capable of being directly compressed into tablets. The invention relates further to a process for preparing the tablets by blending the active ingredient and specific excipients into the new formulations and then directly compressing the formulations into the direct compression tablets. The invention also relates to vildagliptin particle size distribution and a new crystal form of vildagliptin particularly adapted for the preparation of improved tablets and other pharmaceutical compositions.
US20090023683 Complexes comprising zoledronic acid and cyclodextrins The present invention relates to stable compositions comprising zoledronic acid, wherein zoledronic acid is complexed with a cyclodextrin, such as hydroxypropyl-β-cyclodextrin. The invention further relates to processes for making the compositions.
US20090258071 Compositions and methods for ph targeted drug delivery The invention provides compositions and methods for the targeted, in particular, pH targeted, delivery of pharmaceutically active agents in mammals. The compositions comprise pH sensitive diblock copolymers, which permit the release of the pharmaceutically active agent when exposed to an environment having a particular pH. The compositions are particularly useful for the oral delivery of water insoluble pharmaceutically active agents.
WO2008138571A1 Probiotic bacteria containing oral dosage form A nicotine-containing orally administered dosage form useful in smoking cessation therapy wherein said chewing gum comprises probiotic bacteria.
CN102379843A Levocarnitine pharmaceutical composition for injection The invention relates to a stable levocarnitine pharmaceutical composition, and the injection specifically comprises levocarnitine or pharmaceutically acceptable salts thereof and additives for injection, wherein the additives at least contain citrate buffer solution (pH is 6.2), and the other additive is selected from sodium chloride. The levocarnitine injection is good in light resistance, stable in pH, small in skin irritation and easy to realize industrialization.
US8017599 Sequence selective pyrrole and imidazole polyamide metallocomplexes The present invention relates to sequence selective compounds for targeting therapeutic or diagnostic groups to polynucleotides. More particularly, the present invention relates to sequence selective targeting of metallocomplexes, such as metallodrugs and metallodiagnostics, to polynucleotides.
EP2718278A1 Compounds as ppar beta/delta inhibitors for treating ppar beta/delta-mediated diseases The present invention relates to substances that act as selective ligands of nuclear receptors of the PPAR beta/delta subtype and can be used for the treatment of PPAR beta/delta-mediated diseases. The substances of the invention act as inhibitors of the PPAR beta/delta receptor.
CN102727488A Clathrate compound of mesoporous silica/Fe3O4 magnetic nanometer complex and oxaprozin The invention discloses a clathrate compound of a mesoporous silica/Fe3O4 magnetic nanometer complex and oxaprozin. A preparation method for the clathrate compound is as follows: the mesoporous silica/Fe3O4 magnetic nanometer complex is added into an ethanol solution of oxaprozin, wherein a mass ratio of oxaprozin to the mesoporous silica/Fe3O4 magnetic nanometer complex is 1: 1-15; ultrasonic treatment is carried out for 3 to 4 hours; and a resultant is rinsed with secondary distilled water, then separated by using a permanent magnet and finally dried at a temperature of 60 to 75 DEG C for 5 to 7 hours under vacuum so as to obtain the solid clathrate compound. The clathrate compound can be used for preparing oxaprozin targeting medicines, enables the drug that the clathrate compound contains to be located and released at the site of lesion under the influence of an external magnetic field, reduces adverse drug reaction and frequency of administration and allows maximum curative effects of the drug to be performed.
CN101053661A Tetramethylpyrazine derivatives modified silk fibroin protein fiber anti-coagulant material and its preparation method Disclosed are three kinds of ligustrazine derivatives including 2,5-diacryloyl oxymethylene-3,6- dimethylpyrazine, 2-acryloyl oxymethylene-5-methyol-3,6- dimethylpyrazine, and 2- acryloyl oxymethylene-3,5,6- trimethylpyrazine, and three kinds of anticoagulation material modified from three kinds of ligustrazines and obtained on the surface of silk protein fiber by graft polymerization. The invention also provides synthesis of the ligustrazine derivatives and preparation method of the coagulation materials which comprises the steps of transforming the lateral chain of ligustrazine into a ligustrazine derivative with double bond active group and initiating graft polymerization by free radical on the surface of silk protein fiber. The anticoagulation activity of silk protein applied in the biomedical material field is improved and the application field is expanded.
CN103265537A Antitumor compounds, preparation method and application thereof The invention relates to the field of anticancer related medicines, particularly antitumor-activity compounds disclosed as Formula I, and a preparation method, pharmaceutical composition and application thereof.
WO2009072120A1 Use of zinc in combination with chemotherapy for treating cancer The present invention relates to methods for treating cancer using compositions comprising zinc, particularly zinc chloride, in combination with other anticancer agents, comprising administering the compositions to a subject in need thereof by any suitable route of administration other than topical administration.
EP2627340A1 A method of regulating plasma lipoproteins A method of modulating the level of lipoproteins in human cells comprising the step of inhibiting resistin in the cells or cellular environment. The method is useful to treat cardiovascular disease.
US20110313009 Nsaid dose unit formulations with h2-receptor antagonists and methods of use The present invention generally relates to unit dosage forms of naproxen and H2-receptor antagonists, comprising an immediate-release formulation of naproxen; an immediate-release formulation of an H2-receptor antagonist, and a delayed-burst release formulation of an H2-receptor antagonist.
DE102007024802A1 Use of an active substance mixture comprising a fraction specific peptide and fraction essential and non-essential amino acids for the production of a composition to treat, prophylaxis and/or metaphylaxis of e.g. dementia disease Use of a multi-functional active substance mixture comprising a fraction of specific peptide with a molecular weight of up to 10000 Daltons and a fraction of essential and non-essential amino acids, for the production of a composition to treat, prophylaxis and/or metaphylaxis of dementia disease, is claimed, where the mixture is obtained by incubating cells at a suitable growth temperature, subsequently lysing and harvesting together with the preservation medium, separating the cell components, by ultracentrifugation/ultraf iltration, and extracting the fraction of specific peptide and the amino acids. Use of a multi-functional active substance mixture comprising a fraction of specific peptide with a molecular weight of up to 10000 Daltons and a fraction of essential and non-essential amino acids, for the production of a pharmaceutical composition to treat, prophylaxis and/or metaphylaxis of dementia disease, is claimed, where the mixture is obtained by incubating cells at a suitable growth temperature, subsequently lysing and harvesting together with the preservation medium, separating the cell components, which exhibits a molar mass over 10000 Daltons, by ultracentrifugation/ultrafiltration, and extracting the fraction of specific peptide and the fraction of essential and non-essential amino acids. - ACTIVITY : Nootropic; Neuroprotective; Cerebroprotective; Antiparkinsonian; Anticonvulsant. - MECHANISM OF ACTION : None given.
US7425568 Compounds, which are potent inhibitors of Na+ /Ca2+ exchange mechanism and are useful in the treatment of arrhythmias Therapeutically active compounds of formula (I): wherein the variables shown in formula (I) are defined in the disclosure; and pharmaceutically acceptable salts and esters thereof. The compounds are potent inhibitors of the Na+/Ca2+ exchange mechanism.
WO2007114791A1 Lactate and calcium containing pharmaceutical composition and uses thereof The invention relates to a pharmaceutical composition containing 250 to 5000 millimoles per liter of lactate or lactic acid, 0.5 to 1.99 millimoles per liter of calcium and optionally 2 to 10 millimoles per liter of potassium. The invention also relates to pharmaceutical uses of this composition.
CN101676304A Low-molecular-weight glucan, its preparation method and use The invention discloses a low-molecular-weight glucan, characterized in that the glucan is obtained by separating from radix astragali. The invention also discloses a method for separating and purifying the low-molecular-weight glucan. In addition, the invention discloses a use of the low-molecular-weight glucan in the preparation of a medicament for the immunopotentiation and the adjutant therapyof tumor or a health food.
US20110105438 Oligomer-Foscarnet Conjugates The invention relates to (among other things) oligomer-foscarnet conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated foscarnet compounds.
WO2012021647A2 Modulators of nod1 and nod2 signaling, methods of identifying modulators of nod1 and nod2 signaling, and uses thereof Disclosed herein are compositions and methods relating to modulators of Nod-like Receptors NOD1 (NLRC1) and NOD2 (NLRC2) signaling. Further provided are methods of identifying modulators of Nod-like Receptors NOD1 and NOD2 activity. Further provided are compositions and methods for treating or preventing inflammation, including diseases associated with inflammation such as inflammatory bowel diseases (Crohn's disease, ulcerative colitis), pancreatitis, arthritis, asthma, psoriasis, Alzheimer's disease, cardiovascular disease (arteritis), diabetes, and sepsis.
WO2008138079A2 Use of nucleoside derivatives as anti-koi herpes virus in fish The present invention relates to the use of N-phosphonylmethoxyethyl nucleoside analogs for manufacturing a medicament for the treatment or prevention of Koi Herpes virus infections in fish, especially in carps.
CN101091704A Method for preparing medicine dedicated for treating condyloma acuminatum The present invention relates to a special-purpose liquid medicine preparation for effectively curing pointed condyloma. Its preparation method includes the following steps: mixing 35% of bromopropaldehyde, 50% of citric acid and 5% of cathodic-anodic dual-purpose ions, adding 10% of distilled water, standing still for 12 hr, checking purity of said mixed solution, extracting said mixed solution, filling and packaging so as to obtain the invented product.
US20120329872 Ready-To-Eat Feed For Domestic Pets A new finished feed for domestic pets is proposed, containing at least one guanidinoacetic acid component as the active component with regard to nutritional physiology. The new finished feed which preferably has a water content of >8% by weight, can be produced in an extremely economical manner, wherein the main component has a significantly higher stability during passage through the gastrointestinal tract and is therefore only converted into creative under physiological conditions. For this reason the guanidinoacetic acid is also utilized to a high degree by the target group which is in particular cats and dogs.
EP2203439B1 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h, 1'h-ý1, 4'¨bipyridinyl-2'-ones The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
US20090270451 Piperdine Glycine Transporter Inhibitors The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
CN102100805B Composition for relieving physical fatigue and enhancing immunologic function, preparation method thereof and application thereof The invention discloses a composition for relieving physical fatigue and enhancing an immunologic function, a preparation method thereof and application thereof. The composite comprises 10 to 100 weight parts of guarana extract, 100 to 800 weight parts of taurine, 1 to 10 weight parts of L-lysine hydrochloride, 1 to 10 weight parts of L-isoleucine, 0.1 to 5 weight parts of L-leucine, 0.2 to 5 weight parts of L-valine, 1 to 15 weight parts of L-aspartate, 0.01 to 0.3 weight part of L-tryptophan, 0.01 to 0.3 weight part of L-phenylalanine, 0.01 to 0.3 weight part of L-threonine, 0.01 to 0.3 weight part of L-methionine, 10 to 100 weight parts of L-alanine, 10 to 100 weight parts of glycine, 1 to 15 weight parts of tea polyphenol and 1 to 20 weight parts of American ginseng extract.
US20110159091 Rapidly dispersible vaginal tablet that provides a bioadhesive gel A tablet for insertion into a vagina including 0.01 to 500 mg of a vaginal medication, such as a microbicide, such as cellulose acetate 1,2-benzenedicarboxylate (CAP); 100 to 500 mg of mannitol powder; 50 to 300 mg of inert microcrystalline cellulose; 10 to 80 mg of hydroxypropyl methylcellulose; 50 to 250 mg of glycerol and optionally 2 to 4 mg of at least one preservative which protects against microbicidal contamination and discourages the growth of yeast in the vagina. The tablet which includes CAP as the vaginal medication is vaginally administered before coitus in methods for preventing the sexual transmission of HIV-1, HIV-2, herpesvirus, or an infection caused by Neisseria gonorrhoeae, Chlamydia trachomatis, Trichomonas vaginalis, Haemophilus ducreyi or Treponema pallidum. The tablet which includes CAP as the vaginal medication is vaginally administered to prevent or treat bacterial vaginosis.
EP2760842A1 An improved process for the preparation of bendamustine hydrochloride The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1 -Methyl-5-[bis(2-chloroethyl)amino]- 1H-benzimidazol-2-yl]lithium butanoate of formula(V), both having a purity of ≥99%, which is simple, convenient, economical, does not use hazardous chemicals and industrially viable.
WO2009058729A3 Thiazole carboxamide derivatives and their to treat cancer The present invention relates to novel Heterocyclic Ether or Thioether Derivatives, compositions comprising the Heterocyclic Ether or Thioether Derivatives, and methods for using the Heterocyclic Ether or Thioether Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.
US20090074735 Topical product containing sacrificial material for neutralizing free radicals A topical product to protect the skin from free radicals is disclosed in one embodiment of the invention as including a carrier medium for topical application to the skin. A sacrificial material that is compatible with the skin is interspersed with the carrier medium. This sacrificial material may be selected to react with free radicals within the skin. The sacrificial material may be further selected to react with water to produce hydrogen (a powerful antioxidant) and a reaction product that is also compatible with the skin. In this way, both the sacrificial material and the hydrogen will react with free radicals to provide protection against free radicals.
CA2160779C Method and composition for topical treatment of damaged tissue using histamine phosphate as active ingredient A pharmaceutical composition of water, water soluble vinyl polymer gel, amine alcohol dispersant and IEP is used topically to treat herpes labialis and aphthous stomatitis lesions, and also to treat herpes genitalis, chicken pox, allergic conjunctivitis, giant papillary conjunctivitis, stomatitis secondary to chemotherapy, thermal burn, sunburn, decubitus ulcers and shingles.
US20120046353 Cleistocalyx operculatus-derived compounds having inhibitory activities against avian and swine influenza viruses or novel influenza virus The present invention relates to a Cleistocalyx operculatus-derived compound having inhibitory activity against neuraminidase and to a composition for preventing and treating diseases caused by avian and swine influenza viruses and novel influenza viruses, comprising the compound as an active ingredient.
WO2008029300A3 Methods for treating at least one condition having mt1 receptor, 5ht2b receptor, and l-type calcium channel activity The present invention is directed to methods comprising administering a composition comprising a therapeutically effective amount of (R)-verapamil, a derivative thereof, or a pharmaceutically acceptable salt thereof, wherein the composition treats, prevents and/or manages at least one condition having MT1 receptor, 5-HT2B receptor and L-type calcium channel activity and releases the (R)-verapamil, a derivative thereof or a pharmaceutically acceptable salt thereof to exhibit a co-primary activity on the MT1 receptor, the 5-HT2B receptor, and the L- type calcium channel.
US20110262564 Treatment of Cancer with Selenium Nanoparticles Novel chemopreventive and chemotherapeutic cancer treatment method using elemental selenium nanoparticles. Cancer cells, especially androgen dependent prostate cancers are exposed to selenium from elemental selenium nanoparticle treatment, and apoptosis is induced in the cancer cells.
WO2006073359A1 Topical compositions comprising one or more of 44-thiouridine, isomaltitol and uridine The present invention relates to a the use of one or more of the compounds of the group consisting of 4-thiouridine, isomaltitol, and uridine in the preparation of topical, therapeutically effective compositions for treating psoriasis, atopic and contact dermatitis, eczema, seborrhoea, stasis dermatitis and stasis ulcers, as well as allergic rhinitis, as well as a method for treatment of psoriasis, atopic and contact dermatitis, eczema, seborrhoea, stasis dermatitis and stasis ulcers, as well as allergic rhinitis, with the exception of the use of uridine in the treatment of inflammatory conditions caused by bacterial infections.
US20100203051 Diagnostic markers for ankylosing spondylitis and uses thereof Disclosed are methods and agents for detecting the presence or diagnosing the risk of ankylosing spondylitis (AS) in mammals. These methods are based on the detection of polymorphisms within any one or more of the ARTS-1 gene, the IL-23R gene, the TNFR1 gene locus, the TRADD gene locus and the chromosome loci 2P15 and 21Q22. The present invention also features methods for the treatment or prevention of AS based on the diagnosis.
CN101143185A Medicinal composition capable of anti-senility during menopausal syndrome The invention provides an antiaging drug combination for the menopause. The combination consists of active components and medically acceptable complementary materials, wherein the active components consists of the components with the following weight portions of 10 to 31 portions of epimedium herb extracts, 21 to 70 portions of yam extracts and 20 to 50 portions of soybean isoflavone extracts, wherein the epimedium herb extracts contain 20 to 90 percent of total flavones of the epimedium herb; the yam extracts contain 20 to 60 percent of diosgenin; the soybean isoflavone extracts contain 10 to 60 percent of soybean isoflavones. The combination of the invention can protect the women uterus and prevent the osteoporosis and effectively delay the menopause aging of women.
CN102755347A Glucose electrolyte effervescent tablets and preparation method thereof The invention discloses glucose electrolyte effervescent tablets and a preparation method for the glucose electrolyte effervescent tablets. By adopting a polyethylene glycol coating technology, the method is easy and convenient to operate, shortens the production procedure, and is short in production period, safe, easy to control and low in production cost; and the prepared tablets overcome the defect of high osmotic pressure of the conventional oral rehydration salts, improve the taste, can effectively prevent a condition that the oral rehydration salts are rejected due to poor mouthfeel, and are suitable for children.
WO2005023250A1 Use of telmisartan for the prevention of vascular headache The present invention relates to a method for the prophylaxis of vascular headaches which do not originate from hypertension, especially migraine, the method comprising administration of telmisartan to a subject in need of such a treatment. The present invention relates also to a method for the prophylaxis of vascular headaches, comprising the co-administration of telmisartan in combination with other drugs suitable for migraine prophylaxis and/or acute treatment of migraine.
WO2014164526A1 Oxamazin antibiotics Disclosed herein are oxamazin monobactam compounds and their use as antibiotics resistant to degradation by β-lactamases. Also disclosed are pharmaceutical compositions containing the compounds and methods of synthesis.
EP2298332A1 BAFF, inhibitors thereof and their use in the modulation of the B-cell response The invention provides methods for treating or preventing disorders associated with expression of BAFF comprising BAFF and fragments thereof, antibodies, agonists and antagonists.
CN103070840A Oxycodone hydrochloride slow release dripping pills and preparation method thereof The invention relates to the oxycodone hydrochloride slow release dripping pills and a preparation method, and relates to a medicine oxycodone hydrochloride sustained release preparation which can alleviate moderate pain and severe pain and a preparation method thereof. According to the invention, a solid dispersion technology is employed to prepare the slow release dripping pills, the slow release dripping pills are used for solving the disadvantages of low biological availability of oral preparations, and the invention provides the slow release dripping pills with the characteristics of high bioavailability, rapid effect, less administration frequency, convenient administration, less toxic and side effect, convenient storage and transportation and oral administration and the preparation method.
US7169379 Cosmetics The cosmetic of the present invention is a cosmetic that alleviates skin irritation by blending in polypropylene glycol, a specific polar oil, or polybutylene glycol, as well as an ultraviolet absorbent. The present invention also relates to an agent and a method for alleviating irritation by lipophilic drugs. Since the present invention alleviates skin irritation due to ultraviolet absorbents and lipophilic drugs in cosmetics, any amount of ultraviolet absorbents and lipophilic drugs can be blended in cosmetics, and therefore cosmetics that can fully manifest their effects can be provided. Also, it is possible to prepare a safe sunblock cosmetic with superior ultraviolet protection effects because the ultraviolet absorbent is not absorbed through skin.
US20080145377 G-CSF Polypeptides And Uses Thereof The present invention relates to G-CSF polypeptides and their uses, particularly for therapeutic or prophylactic treatment in human subjects. The invention also relates to nucleic acids encoding said polypeptides, vectors comprising such nucleic acids and recombinant cells containing the same. The invention further discloses methods of producing such polypeptides, as well as methods and tools for detecting or dosing these polypeptides in any sample.
CN1634007A Benzalkonium chloride contraceptive gel for quick eradication of multiple venereal disease pathogenic organism The invention provides a Benzalkonium chloride contraceptive gel for quick eradication of multiple venereal disease pathogenic organism which comprises the following compositions (by weight ratio), dodecyl dimethyl benzyl ammonium chloride 0.1-5%, hydroxyl propyl methylcellulose 0.5-5%, hydroxyl benzoate 0.1-4%, and deionized water 30-96%. The invention can be applied for both contraception and prevention of venereal disease infection.
US20100286255 Method for extracting secoisolariciresinol and dihydroquercetin from wood The invention relates to extracting secoisolariciresinol and dihydroquercetin from wood. The inventive method consists in extracting disintegrating wood of a screen area by means of a non-splitting mixture of organic solvent and water, the solvent content ranging from 50 to 75%, in such a way that a secoisolariciresinol and dihydroquercetin-containing extract is obtained, and in processing said extract by removing the solvent in such a way that a final secoisolariciresinol and dihydroquercetin-containing mixture is obtained. In the other variant, the inventive method consists in extracting disintegrating wood of a screen area by means of a non-splitting mixture of organic solvent and water, the solvent content ranging from 50 to 75%, in such a way that a secoisolariciresinol and dihydroquercetin-containing extract is obtained, in processing said extract by removing the solvent in such a way that a final secoisolariciresinol and dihydroquercetin-containing mixture is obtained and in exposing the thus obtained mixture to selective extraction and crystallization in such a way that secoisolariciresinol and dihydroquercetin are extracted. In the third variant, the inventive method consists in extracting disintegrating wood of a screen area by means of a non-splitting mixture of organic solvent and water, the solvent content ranging from 50 to 75%, in such a way that an secoisolariciresinol and dihydroquercetin-containing extract is obtained, in processing said extract by removing non-polar components, in removing supernatant liquid, in chromatographing the obtained residue on a silica gel layer and in removing an eluent in such a way that a dry secoisolariciresinol and dihydroquercetin mixture is obtained. The use of secoisolariciresinol and dihydroquercetin in the form of components of biologically active additives and chemical-pharmaceutical products is also disclosed.
WO2013170671A1 Pteridine ketone derivative and applications thereof as egfr, blk, and flt3 inhibitor Provided are a pteridine ketone derivative used as an EGFR, BLK, and FLT3 inhibitor and applications thereof. Specifically, provided are a compound of the following formula I, a pharmaceutical composition containing the compound of the formula I, and use of compound in preparing medicine for treating diseases mediated by EGFR, BLK, or FLT3 or inhibiting EGFR, BLK, and FLT3.
CN101669973A Biological immunopotentiator composition for treating cancers The invention relates to a biological immunopotentiator composition for treating cancers. The composition medicament for treating the cancers mainly comprises 0.5 to 15 billions of inactivated human salmonella typhi, 1 to 10 billions of inactivated bordetella pertussis, and diphtheria toxoid, tetanus toxoid or staphylococcus aureus enterotoxin C. The novel composition is helpful for activating the immune system of a tumor patient, improving the quality of life, and inhibiting tumor growth and metastasis.
WO2011049327A3 A skin external composition comprising a salt and sugar as active ingredients for preventing and treating vaginosis and the use thereof Present invention relates to a skin external composition comprising a combination of salt and sugar as an active ingredient in an amount effective to treat or prevent vaginosis, together with a pharmaceutically acceptable carrier and the use thereof.
US20080312326 Method for the Prevention and/or Treatment of Neurodegenerative Diseases Characterized by Administering and Ep1 Receptor Antagonist The present invention relates to the use of EP1 receptor antagonists for the treatment of neurodegenerative diseases, for example, Alzheimer's disease, Parkinson's disease, Parkinson syndrome, dementia, amyotrophic lateral sclerosis, progressive supranuclear palsy, Huntington's disease, spinocerebellar ataxia, etc.
WO2008116391A1 The neuroblast proliferation promoter and the neurite outgrowth promoter A neuroblast proliferation promoter comprising phenylethanol glycoside compounds or the extract of Cistanche, which can promote the proliferation of neuroblast and the outgrowth of neurite of neuroblast at the condition of neuroblast having no disorder. The neuroblast proliferation promoter can be used to prepare medicine, the external formulation for skin, the food for drinking and the feed for mammal.
EP2712615A1 Composition containing arylnaphthalene lignan derivative for preventing and/or treating dementia A composition for preventing and/or treating dementia and ameliorating memory impairment and/or improving memory, comprising one or more arylnaphthalene lignan derivatives, such as Justicidin A, 5-methoxyjusticidin A, Chinensinaphthol, and a pharmaceutically-acceptable salt thereof, as active ingredient.
CN102584916A Lignan triglucoside compound and preparation method and application thereof The invention discloses a lignan triglucoside compound and a preparation method and application thereof. The molecular formula of the lignan triglucoside compound is C38H54O21. The preparation method for the lignan triglucoside compound comprises the following steps of: extracting crushed Castanea henryi (Skan) Rehd. et Wils shells in an organic solvent, separating to obtain leaching liquor, extracting the leaching liquor, and concentrating the extracted liquor to obtain an extract; and performing chromatographic separation and purification on the extract, and thus obtaining the lignan triglucoside compound, wherein the organic solvent is one or more of methanol, ethanol, n-butanol and acetone. The lignan triglucoside compound with a novel structure is extracted and separated from the Castanea henryi (Skan) Rehd. et Wils shells; and the compound has good tyrosinase inhibiting activity, can be used for preparing tyrosinase inhibiting medicaments, whitening cosmetics or whitening health-care food, and has a good development prospect.
US20100305183 Method and composition for reducing reperfusion injury The present invention relates to a method of preventing and/or reducing reperfusion injury to a tissue, organ, or organ system in a subject. The method includes administering to the subject an effective amount of a substance P receptor antagonist.
CN101153044A Wide-spectrum antibiotic cephalosporin alkene compounds containing sulfhydryl thiazole pyridine onium methyl The present invention discloses a cephalosporin compound, a representative of the general formula (I). Wherein, X represents N or CY (wherein, Y represents H or halogen); R1 represents amino or freely chosen protective amino; R2 represents H, alkyl, freely chosen low-grade alkyl for substitution and so on; R3 represents alkyl, alkenyl, freely chosen low-grade alkyl for substitution and so on; the wave line of the general formula (I) represents sequential, reversed isomer or the mixture. The present invention also discloses the preparation method, drug compositions containing the compound, and the application of the compound in preparing drugs of broad-spectrum antimicrobial functions to various pathogenic bacteria.
US20130012589 Stable aqueous formulation of (e)-4-carboxystyryl-4-chlorobenzyl sulfone An aqueous pharmaceutical solution composition comprising between about 20 mg/ml to about 100 mg/ml of a radioprotective α,β-unsaturated aryl sulfone, a cosolvent comprising polyethylene glycol (PEG), polypropylene glycol, polyglycerol, DMA, propylene glycol, glycerol, ethanol, sorbitol, isopropyl alcohol, or a combination thereof in an amount between about 25% and about 90% w/v, and a water soluble Vitamin E derivative, wherein the composition has a pH within the range of about 7.0 to about 9.5.
EP2743255A1 Cocrystal of agomelatine with phosphoric acid The present application relates to cocrystal of agomelatine with phosphoric acid and its method of preparation. Another aspect of the application relates to process for the preparation of crystalline Form I of agomelatine.
US20120100077 Mixture of amphipathic molecules and method for modifying cell membranes by means of fusion Disclosed is a mixture of amphipathic molecules and a method for modifying cells in vivo by way of membrane fusion with these molecules.
US20080221110 Tricyclic condensed ring nitrogen compound selectively acts on cannabinoid receptors; Gram-negative and Gram-positive bacterial infections; 1-({4-[(6,7-Dihydro[1,4]dioxino[2,3-c]pyridazin-3-ylmethyl)amino]-1-piperidinyl}methyl)-9-fluoro-1,2-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one Tricyclic nitrogen containing compounds and their use as antibacterials
US7329777 Methods for treating heart failure, thromboembolic disorders, and pulmonary fibrosis This invention relates to methods for treating heart failure, thromboembolic disorders, and pulmonary fibrosis, comprising administering an effective amount of a compound of formula (I) in which the several variables are as defined in the specification and claims.
WO2013081563A3 Stable voglibose tablet formulations The present invention relates to voglibose tablet formulations comprising at least one pharmaceutically acceptable diluent.
CA2537820C Process for preparing water-soluble medicaments comprising complexation of forskolin in cyclodextrins Aqueous solutions of diterpenes such as Forskolin, its congeners, analogs and derivatives, up to approximately 6% concentration, are prepared using suitably substituted cyclodextrin as a solubilizing agents. In the absence of cyclodextrin, some diterpenes such as Forskolin are soluble in water only to concentrations of about 0.001 % .Such aqueous solutions find applications in topical and systemic use, as pharmaceutical, cosmeceutical, nutraceutical preparations containing diterpenes such as Forskolin and congeners.
EP2041151B1 A method of preparing a glycoside of a mono- or diacylglycerol product from a plant material The present invention provides a method of preparing a glycoside of a mono- or diacylglycerol product from a plant material. The method comprises the steps of: (i) optionally milling the plant material, (ii) extracting the optionally milled plant material with a first aqueous extraction solution obtaining a first liquid phase and a first solid phase, (iii) separating the liquid phase from the solid phase to obtain a glycoside of mono- or diacylglycerol product, (iv) extracting the solid phase from step (iii) with a second ex- traction solution obtaining a second liquid phase and a second solid phase, and (v) separating the second liquid phase from the second solid phase to obtain a second and a third glycoside of mono- or diacylglycerol product, wherein the second extraction solution further comprises a cell wall degrading enzyme or a mixture of cell wall degrading enzymes.
US20080090841 pyrazinoylguanidine derivatives; more potent, more specific, and/or absorbed less rapidly from mucosal surfaces, and/or are less reversible, give a prolonged pharmacodynamic half-life; treating anthrax, chronic bronchitis, cystic fibrosis,chronic obstructive pulmonary disease, emphysema, pneumonia The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium channel blocker as defined herein and an osmolyte to a subject to a subject in need of increased mucociliary clearance and mucosal hydration.
CN102078308A Aspirin lysine dispersible tablet and preparation method thereof The invention provides a novel aspirin lysine dispersible tablet, which is prepared from the raw drugs in parts by weight: 0.25-1 of aspirin lysine, 0.1-10 of filling agent, 0.1-10 of disintegrating agent, 0.01-0.5 of flavoring agents, 0.01-0.2 of adhesives, 0.1-5 of fluidizers and 0.01-1 of essences. The invention also provides a preparation method of the novel aspirin lysine dispersible tablet. The aspirin dispersible tablet provided by the invention quickly disintegrates and releases when contacting with the water so as to form a sweet-taste solution, and the solution can be orally taken directly or taken after dissolving with the water. The novel aspirin lysine dispersible tablet solves the problems of easiness of degradation of free salicylic acid in aspirin lysine, improves the stability of aspirin lysine medicines, is convenient for carrying and taking, is suitable for patients who are difficult to swallow, and also can be orally taken directly (small specification of tablets), in particular to children, thereby the compliance of taking the medicine can be improved.
WO2014134232A1 Carbazole compounds useful as bromodomain inhibitors The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
EP2319516A1 Compounds for treating inflammatory and autoimmune disorders The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
US7211571 Composition for the prevention and/or treatment of lipid metabolism disorders and allergic forms A composition is disclosed which can be used as a health food/dietary supplement or as a drug for the prevention and/or treatment of lipid metabolism disorders and allergic forms and for activating organic defences against infections and tumor processes, containing as its characterizing components isovaleryl L-carnitine and a polysaccharide selected from glucans and galactans.
WO2010143075A3 Silver hydrosol, dental applications and other uses thereof Microbiologically effective silver hydrosol is used to reduce the local level of microorganisms at the site of a dental procedure and to prevent or inhibit their growth during the healing that follows the procedure. Any gingival lesions created by a dental procedure are treated with silver hydrosol in an aqueous gel. Following the procedure the patient's mouth is periodically rinsed several times a day with a solution of silver hydrosol or, more preferably, with a combination of silver hydrosol and hydrogen peroxide. These steps result in a significant reduction in post operative pain and swelling. Overall healing is accelerated by this treatment.
WO2007100091A1 Composition for suppressing the expression of fucosyltransferase Disclosed is a means for reducing the expression amount of a FUT8 gene, reducing the expression amount of a FUT8 protein, and/or reducing the expression amount of a product produced by the action of FUT8.
US20090170951 Phenolic Hydrazone Macrophage Migration Inhibitory Factor Inhibitors Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.
CN102172348A Solid oseltamivir phosphate medicinal composition The invention provides a powdered oseltamivir phosphate medicinal composition, which comprises a therapeutic or prevention effective amount of oseltamivir phosphate, sodium glutamate and any one or more pharmaceutically acceptable excipients. The invention also provides the use of the solid medicinal composition in the preparation of oral liquid medicines and further provides a liquid medicinal composition which comprises the solid medicinal composition provided by the invention and a water-containing medium. When prepared into suspension with water, the solid medicinal composition has a stable advantage.
US20050031696 Oral pharmaceutical formulations of acid-labile active ingredients and process for making same An oral pharmaceutical formulation in dosage form of acid-labile compounds, methods of treating using the formulation and a process for its production are described.
EP2295051A1 Wound healing compound Wound healing composition comprises lime permeated into liquid, and oil, which are mixed together. An independent claim is also included for producing the wound healing composition, comprising providing limestone, mixing lime and liquid in a container and mixing the oil. - ACTIVITY : Vulnerary. No biological data given. - MECHANISM OF ACTION : None given.
US20110218181 Formulations of deoxycholic acid and salts thereof The present application is directed to an aqueous pharmaceutical formulation comprising less than about 5% w/v sodium deoxycholate maintained at a pH sufficient to substantially inhibit precipitation of the sodium deoxycholate. Also disclosed herein, are methods for inhibiting precipitation of sodium deoxycholate in an aqueous solution comprising less than about 5% w/v of sodium deoxycholate, said method comprising maintaining pH of the solution of from at least about 8.0 to about 8.5.
WO2006099474A1 'n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamides metabolites The present invention is directed to metabolites of 'N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarbo xamide, the compound of formula (I), pharmaceutical compositions thereof, and to methods of using the metabolites and the pharmaceutical compositions in the treatment of oncological and immunological disorders. [PLEASE INSERT CHEMICAL STRUCTURE HERE] (I)
CN101260091A Acrylamides compounds containing 1,2,3-thiadiazoles ring and having anti-hepatitis B virus activity The invention relates to an acryl-amide compound containing 1, 2 and 3-oxadiazole ring and anti-HBV activity and the application of the same, which is a compound as the structural formula(I) on the right side, wherein X indicates hydrogen or halogen; R1 indicates an amino group, 1-6 carbon alkyl amino, arylamine, Morpholine or Pip; when R3 is 4-methyl-1, 2 and 3- oxadiazole-5-group, R2 indicates Phenyl and substituted Phenyl; when R2 is 4-methyl-1-oxadiazole-5-group, R3 indicates Phenyl and substituted Phenyl. The acryl-amide compound is an anti-HBV activity compound, shows extremely high activity in the inspection of anti-HBV replication and can be further used to manufacture drug that can treat and/or prevent Hepatitis B.
WO2009053732A1 Novel salt The present invention relates to a novel salt of tegaserod, namely the dihydrogen phosphate salt. The present invention also relates to novel amorphous and crystalline forms of the dihydrogen phosphate salt of tegaserod. The invention further relates to processes for the preparation of the novel salt and the novel amorphous and crystalline forms. The invention also relates to pharmaceutical compositions containing the novel salt or the novel amorphous or crystalline forms, and to uses of said compositions to provide methods of treating patients suffering from gastrointestinal disorders.
EP1556362B1 Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
WO2009065604A3 Pharmaceutical composition comprising glucosamine sulfate, chondroitine sulfate and ibuprofene The present invention relates to the field of medicine and, more particularly, to drugs for internal use to treat a pain syndrome during a pain exacerbation phase in primary osteoarthrosis and secondary osteoarthrosis and other degenerative dystrophic diseases of extremity joints and intervertebral disks. The pharmaceutical composition for oral administration comprises chondroitin sulfate salt and glycosamine sulfate salt, ibuprofen as a nonsteroidal anti-inflammatory drug, and auxiliary substances wherein the ingredients are comprised in the following ingredient ratio (% w/w): Chondroitin sulfate salt 20 to 30 Glucosamine sulfate salt 30 to 36 Ibuprofen 10 to 15 and auxiliary substances Q. S. The present invention provides a pharmaceutical composition which ensures a chondroprotective, anti-inflammatory, and analgetic effect, an effective treatment of degenerative dystrophic diseases of extremity joints and intervertebral disks, a convenience of using the medicine, decrease in side effect risks, and the provision of an alternative medicament.
US20120128670 mTOR INHIBITOR AND ANGIOGENESIS INHIBITOR COMBINATION THERAPY Cancer therapy comprising treatment with an mTOR inhibitor, such as a dual mTORC1/mTORC2 inhibitor, such as OSI-027, in combination with an angiogenesis inhibitor.
CN1812796B Aivlosin for the treatment of disease due to brachyspira pilosicoli or ornithobacterium rhinotracheale The invention relates to the use of Aivlosin for the treatment, prevention or control of diseases due to Brachyspira pilosicoli in pigs and Ornithobacterium rhinotrachelae in poultry.
CN101406463A Method for preparing metronidazole, clotrimazole and chlorhexidime vaginal acetate effervescent tablet and quality control method The invention relates to a method for preparing a new gynecological anti-bacterial anti-inflammatory drug, namely dithiazole vaginal effervescent tablet and a method for quality control. The dithiazole vaginal effervescent tablet is used for treating gynecopathy, anorectal diseases and skin commonly-encountered diseases such as pelvic inflammatory disease, cervical erosion, vaginitis and the like caused by anaerobic bacteria, aerobic bacteria, trichomoniasis, pure or mixed fungal infections. The dithiazole vaginal effervescent tablet is characterized in that lactic acid and a calcium lactate buffer system are added to the formulation so that the pH value of the drug is between 3.5 and 4.0 similar to the vaginal physiological pH and is advantageous to remove pathogen and infusorian, provide living conditions suitable for vaginal beneficial bacterium group of lactic acid bacteria, and promote the illness rehabilitation. Besides, the dithiazole vaginal effervescent tablet uses pharmaceutical acceptable water-soluble polymer materials such as water-soluble polymer polyethylene glycol, polyvidone K30 and the like to enwrap acidic or alkaline components of an effervescent disintegrant so as to avoid the occurrence of hidden spots or even collapsing phenomenon on the surface of the tablet caused by gas production reaction resulted from small amount of water in the storage process, and uses a ethanol solution with adhesives and surface-active agents for granulation so that the hydrolysis of clotrimazole can be prevented, the infiltration of moisture is promoted in use, the uniform collapse is accelerated, and gas bubbles are homogeneous and stable.
US7087579 Human sodium glucose co-transporter 2 (SGLT2) inhibitors; hypoglycemic agents, antidiabetic agents; obesity; prodrugs The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.
CN101596197A Quick-release medicinal composition and preparation method thereof The invention relates to a quick-release medicinal composition, which contains indiplon and pharmaceutically acceptable carrier. The oral quick-release composition prepared from the indiplon and the quick-release carrier can provide a new convenient medicament administration mode and a new dosage form for oral medicaments under the special conditions that the medicaments are difficult to swallow and inconvenient to drink water. Compared with a common oral preparation, because the mucosa of the gastrointestinal tract is widely covered by rapidly-disintegrated medicament, the medicinal composition has quick response. If the medicament can be absorbed through the mucosa of the oral cavity, the medicinal composition has no first-pass effect so as to improve the bioavailability and reduce the stimulation to the stomach and intestine.
EP1495322A2 Heteroclitic analogs and related methods Heteroclitic analogs of class I epitopes are prepared by providing convervative, semi-conservative, or non-conservative amino acid substitutions at positions 3 and/or 4 and/or 5 and/or 6 and/or 7 and/or 8 and/or 9 and/or 10 of these epitopes. The analogs are useful in eliciting immune responses with respect to the corresponding wild-type epitopes.
CN103083666A Drug composition, drug composition preparation and drug composition uses The invention belongs to the technical field of medicine, and discloses a drug composition comprising (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-yl pyrimidine-2-yl)amino]phenyl)-2,3-dihydro-inden-5-amide sesquisulfate and chlormethine in a DNA alkylated cross-linking agent, wherein the drug composition is determined through scientific experiments, test results show that the chlormethine in the DNA alkylation cross-linking agent does not affect compound stability, and pharmacological test results show that the (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-yl pyrimidine-2-yl)amino]phenyl)-2,3-dihydro-inden-5-amide sesquisulfate and the chlormethine provide a synergistic effect.
CN1742744A Compound licorice acid monoamine powder injecta and preparing method The present invention relates to a compound monoammonium glycyrrhizinate powder injection preparation and its preparation method. It is made up by using monoammonium glycyrrhizinate, glycine and L-cysteine hydrochloride and adding proper quantity of sterile water for injection and auxiliary material. Said invention has the effects of resisting virus, regulting immunity, protecting membrane structure, resisting ulcer and relieving spasm, and can obtain good therapeutic effect for curing virus hepatitis.
WO2009152167A2 Delivery of therapeutics The present invention provides materials and devices for the controlled release of therapeutics, and methods for uses thereof.
US20080058293 Quinoline Derivates and Their Use in Therapy The invention provides compounds of formula (I) wherein n, p, q, X, R1, R2, R3, R4, R5 and R6 are as defined in the specification; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
EP2773358A1 Compositions and methods for hemostasis The present invention relates to water soluble and completely absorbable and/or physiologically degradable hemostatic compositions having a wax or wax-like base effective for use in tamponade hemostasis of bone or cartilage.
CN103356743A Natural medicinal composition, its preparation method and application The invention relates to a natural medicinal composition, its preparation method and application. The natural medicinal composition consists of a cinnamon gallnut decocted concentrated extract, cinnamaldehyde and a gallnut acetone extract in a ratio of 4-7:3-4:5-9. The composition provided in the invention has excellent efficacy on cancer chemotherapy related diarrhea and simultaneously has a synergistic effect on cancer chemotherapy..
WO2007121662A1 Diphenyl urea derivatives as kinase inhibitors, compositions and uses thereof The present application discloses the diphenyl urea derivatives of general formula (I), pharmaceutically acceptable salts, solvates or prodrugs thereof. The present compounds have the effective bioactivities in inhibiting the VEGFR2 and/or PDGRFβ.
WO2009079765A1 Compounds with activity at the 5-ht2c receptor A compound of Formula (I): wherein R1 is a substituted or unsubstituted heterocycloalkyl containing at least two rings, wherein said rings are fused rings, bridged fused rings and/or spiro rings. A method for treating a 5-HT2C receptor-mediated disorder in a mammal using the same.
WO2008117970A1 Use of inhibitors of leukotriene b4 receptor blt2 for treating human cancers The present invention relates to a new use of inhibitors of leukotriene B4 receptor BLT2 for treating human cancers. More particularly, the present invention relates to a pharmaceutical composition for treating human cancers comprising BLT2 inhibitors and a method for treating human cancers using BLT2 inhibitors. The present inventors revealed the role of BLT2 as a survival factor of human cancers, such as bladder, prostate, pancreatic, and breast cancer and found that the BLT2 inhibitors can be used as anti-cancer drugs. The present inventors revealed that BLT2 has an important role in metastasis of cancer cells and angiogenesis of tumor and demonstrated that the anti-cancer activity of the BLT2 inhibitors is accomplished by inducing the apoptosis of cancer cells, inhibiting the metastasis of cancer cells, or inhibiting the angiogenesis of tumor.
US7119074 Treatment of cancers, tumors and malignancies using amphiphilic prodrugs The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.
US7030246 Tetrahydroquinoline derivatives as stat6-modulators, preparation and use thereof Compounds of formula (I) are modulators of STAT6 signal pathway activity, and can be used in the treatment of atopic dermatitis, urticaria, allergic asthma, allergic rhinitis, a food allergy, allergic conjunctivitis, hayfever, bullous pemphigoid, industrial sensitization, chronic rejection of transplants or COPD
CN1785203A Astragaloside cyclodextrin clathrate, its prepn. and preparing mehtod An inclusion compound used as medicine is prepared from astragaloside A and cyclodextrin through including the astragaloside A by cyclodextrin. Its preparing process is also disclosed. It has the improved solubility and biological utilization rate.
WO2006059423A1 Medicine for treatment of disease caused by hyperstimulatory cytotoxicity and therapeutic method A medicine for treatment of diseases (for example, ischemic cerebrovascular disease) caused by hyperstimulatory cytotoxicity through protection or relief against hyperstimulatory cytotoxicity (for example, neurocytotoxicity); and a relevant therapeutic method. Further, there are provided a method of assessing any hyperstimulatory cytotoxicity and a method of screening a factor capable of inhibiting the cytotoxicity.
WO2014044113A1 Pyrazol[3,4-c] pyridine derivative, preparation method and use in medicine thereof Disclosed is a pyrazol[3,4-c] pyridine derivative, preparation method thereof and a pharmaceutical composition comprising the derivative and use thereof as a therapeutic agent, especially as Xa factor inhibitors in the preparation of drugs for treating diseases like thromboembolism.
US20080004320 Remedy for Glomerular Disease Provided is a pharmaceutical composition useful for the prevention or therapy of glomerular diseases, in particular progressive chronic glomerular diseases. A preventive or therapeutic agent for a glomerular disease containing pyridoxamine or a salt thereof, and an angiotensin II receptor antagonist.
WO2014079805A1 Pyrazole compounds for treating hairloss The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof for use in the treatment or prevention of hairloss, wherein W, L1, L2, X, L3, Y, R1 and R2 have one of the meanings as indicated in the specification and claims, to pharmaceutical compositions containing said compounds or pharmaceutically acceptable salts thereof, to the use of said compounds or pharmaceutically acceptable salts thereof for the manufacture of a medicament useful for the treatment or prevention of hairloss, to a method of treating or preventing hairloss as well as to a method of stimulating hair growth.
US20090291916 Trihydroxy Polyunsaturated Eicosanoid The invention features methods for the preparation of naturally occurring trihydroxy polyunsaturated eicosanoids and their structural analogs. The invention further provides new derivatives and analogs of trihydroxy polyunsaturated eicosanoids that can be prepared according to these methods. The invention also provides compositions and methods using trihydroxy polyunsaturated eicosanoid derivatives for the prevention, amelioration and treatment of a variety of diseases or conditions associated with inflammation or inflammatory response, autoimmune diseases, rheumatoid arthritis, cardiovascular diseases, or abnormal cell proliferation or cancer.
WO2008023273A3 Method for improving pharmacokinetics The present invention provides pharmaceutical compositions and methods for improving the pharmacokinetics of drugs which may be metabolized by cytochrome P450 monooxigenase, the method may comprise co-administering a compound of formula (I), with the drug; when the compound of formula (I) comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, H, (HO)2P(O)-, (NaO)2P(O)-, alkyl-CO- or cycloalkyl-CO-, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.
US20080213166 Novel Gene Targets and Ligands that Bind Thereto for Treatment and Diagnosis of Colon Carcinomas Isolated nucleic acids and proteins that are overexpressed in human cancers, and antibodies that specifically bind the proteins, which are useful diagnostic and therapeutic targets.
CN103169693A Application of wogonin derivant in preparation of drug for treating liver cancer The invention provides application of a compound shown in a formula I in preparation of a drug for treating liver cancer. The drug composition provided by the invention contains the compound shown in the formula I and one or more pharmaceutically acceptable carriers, wherein the compound in the formula I exerts the anti-tumor effect by inducing cell apoptosis.
CN1803837B Neurotrophic growth factor There is disclosed an isolated nucleic acid molecule encoding a human neurotrophic growth factor designated enovin and having the amino acid sequence illustrated in Figure 1, 21, 23 or 24 or encoding a functional equivalent, derivative or bioprecursor of said growth factor. The growth factor preferably comprises the amino acid sequence from position 27 to 139 of the sequence illustrated in Figure1, or a functional equivalent, derivative or bioprecursor thereof. The nucleic acid molecule encoding enovin can be used to transform a host cell, tissue or organism by including it in an appropriatevector. The host cell, tissue or organism and the vector also form part of the invention.
CN103040767A Stable kalii dehydrographolidi succinas freeze-dried powder injection for injection The invention provides a stable kalii dehydrographolidi succinas freeze-dried powder injection for injection, and in particular provides a kalii dehydrographolidi succinas freeze-dried powder injection. The kalii dehydrographolidi succinas freeze-dried powder injection comprises kalii dehydrographolidi succinas, alkali metal salt and an optional pharmaceutical acceptable auxiliary material. The stable kalii dehydrographolidi succinas freeze-dried powder injection for injection is applicable to treatment of diseases such as viral pneumonia and viral upper respiratory tract infection. The powder injection is excellent in pharmaceutical performances such as the stability, thus providing a safe, efficient and controllable antiviral drug for clinic.
CN102846568A Preparation method of cephalexin layering digestion tablet A preparation method of a cephalexin layering digestion tablet comprises the steps of: taking 1.5kg from 13kg of starch to prepare a starch paste with concentration of 12% as a binder; mixing the remaining starch with the binder, and pressing a substrate with weight of 0.13g and diameter of 6.5-7mm; mixing a bulk medicine cefalexin powder with a lubricant to obtain a mixed powder; placing the prepared substrate in a sugar-coating pot, spraying 12kg of mixed powder on the substrate layer by layer by a spray gun with a sodium carboxymethyl cellulose solution as a spray, drying, and airing the tablet, so as to obtain the cephalexin layering digestion tablet. The invention has the advantages that starch is used to suppress substrate, and the bulk medicine is sprayed on the substrate, so as to facilitate drug disintegration, and avoid impediment on digestion speed of the bulk medicine by adjuvant materials for mixing tabletting; and the drug has good digestion speed, can digest more than 90% of the total drug in 15 seconds, and quickly reach blood drug level threshold required by treatment in the human body, and has good treatment effect.
WO2010077663A2 Substituted tetracyclic 1h-indeno (1,2-b) pyridine-2 (5h)-one analogs thereof and uses thereof Provided herein are tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analogs and derivatives, compositions comprising an effective amount of a tetracyclic 1H- indeno[1,2-b]pyridine-2(5H)-one analog and/or derivative and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, a reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, an ocular or ophthalmologic disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, contrast induced nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of a tetracyclic 1H- indeno[1,2-b]pyridine-2(5H)-one analog or derivative.
EP1805172A1 4-methoxymethyl-pyrrolidine-2-carboxylic acid compounds and derivatives thereof as hepatitis c virus inhibitors Anti-viral agents of Formula (la) wherein: A represents hydroxy; D represents 4-tert-butyl-3-methoxyphenyl; E represents 1,3-thiazol-2-yl or 5-methyl-1,3-thiazol-2-yl; G represents methoxymethyl; J represents 1,3 thiazol-2-ylmethyl, 1,3-thiazol-4-ylmethyl, 1,2-thiazol-3-ylmethyl, or 1H-pyrazol-1-ylmethyl; and salts, solvates and esters thereof; provided that when A is esterified to form -OR where R is selected from straight or branched chain alkyl, aralkyl, aryloxyalkyl, or aryl, then R is other than tert-butyl; processes for their preparation and their use in HCV treatment are provided.
US20090081194 Compositions and methods for reducing risk of development, or severity, of inappropriate immune response in eyes A composition for reducing the risk of development, or severity, of an inappropriate immune response in an eye comprises an antagonist to at least a human TLR, an antagonist to at least a coreceptor of human TLR, a compound that is capable of inhibiting an activation of a human TLR signaling pathway, or a combination thereof. The composition can be used to reduce the risk of development, or severity, of contact lens-associated corneal infiltrates. The composition can be formulated into an eye drop or a contact lens-treating, -storing, -cleaning, -disinfecting, or -wetting solution.
US8252524 Method of screening pharmaceutical compositions that promote nuclear transfer of Cdc42 protein A nuclear transfer promoter for Cdc42 protein comprising an isoprenoid synthesis inhibitor and/or a geranylgeranyl transferase inhibitor such as an HMG-CoA synthase inhibitor, an HMG-CoA reductase inhibitor, an AMPK activator or a farnesyl pyrophosphoric acid synthase preparation; utilization thereof; a method therefor; a blood vessel remedy comprising the nuclear transfer promoter for Cdc42 protein as the active ingredient; and a method of screening a blood vessel remedy which comprises assaying the ability of Cdc42 protein to transfer into nucleus.
CN102698271A Hypoglycemic drug composition and application of hypoglycemic drug composition The invention relates to a hypoglycemic drug composition, which contains alpha-glucosaccharase inhibitor and Indian Trumetflower Seed extract, wherein the Indian Trumetflower Seed extract is prepared by the processes of extracting the Indian Trumetflower Seed with aqueous solution of organic solvent, filtering, re-extracting, separating and drying. The drug composition prepared from the Indian Trumetflower Seed extract and alpha-glucosaccharase inhibitor lower than normal dosage has excellent hypoglycemic effect. The hypoglycemic drug composition has the main advantages that postprandial blood glucose can be reduced faster and more efficiently, and less alpha-glucosaccharase inhibitor is used, so the drug effect can be improved, the toxic and side effects of the alpha-glucosaccharase inhibitor are effectively reduced, and the problems of hypoglycemia and the like easily caused by drug combination are also effectively solved.
CN102895612A Preparation technology of integrated novel preparation of yuebi pinellia decoction The invention relates to a preparation technology of an integrated novel preparation of yuebi pinellia decoction, comprising the following herbs as effective ingredients: 10 weight parts of ephedra, 30 parts of gypsum, 6 parts of ginger, 6 parts of licorice, 12 parts of jujube, and 15 parts of pinellia. The preparation process comprises the following steps: conducting supersonic airflow grinding, alcohol and aqua abstraction, supersonic shattering extraction, decocting for concentration, supersonic spray drying, nanogrinding, high-pressure homogenization, nanoparticle preparation, etc. According to the invention, the advantages of multi-synergy and multi-targets reflected in nanocarrier combined technology are utilized herein; after large-scale production, the production cost can be greatly reduced, the product quality can be greatly raised, and the drug targeting and slow releasing action are improved; the decoction preparation disclosed herein can be taken internally and externally and can be respectively taken for 4 periods of time according to midnight-midday ebb flow and qi and blood flow rules of human body; the decoction preparation disclosed herein can be prepared into a film-forming agent and a transdermal agent, can be respectively applied on different parts of human body according to the midnight-midday ebb flow and qi and blood flow rules of human body, and can be adsorbed directly through skins.
WO2012105887A1 Active principle for mitigating undesired medical conditions A composition for treating or preventing inflammatory-related conditions which comprises as an active principle (= AP) a carrier which exhibits a plurality of a scavenger structure which is capable of mitigating the activity of a mediator of inflammatory-related conditions. The scavenger structure comprises a nucleophilic centre complying with the formula (I); a) X1 is a single-bonded heteroatom selected amongst N, O and S and exhibits a free electron pair, b) m is 0 or 1 and n is 1 or 2, c) -R"- is a bivalent organic group providing attachment to the carrier via one of its free valences and to X1 at the other free valence, and d) R'- is a monovalent organic group attached to the X1 via its free valence. A method for treating or preventing inflammatory-related conditions in an individual suffering from or being at risk for such conditions. The method comprises the steps of: i) providing the composition of the invention containing AP, and ii) contacting AP with said mediator a) within said individual, or b) separate from said individual.
CN101721378A Method for preparing cefmenoxime hydrochloride freeze-dried powder injection The invention discloses a method for preparing a cefmenoxime hydrochloride freeze-dried powder injection, which comprises the following steps of: dissolving cefmenoxime hydrochloride and arginine together; quickly cooling and freezing solution decolorized by activated carbon in a freeze dryer; vacuumizing; and gradually raising the temperature to room temperature. The obtained cefmenoxime hydrochloride freeze-dried powder injection has the advantages of over 98 percent of average yield, less than 0.5 percent of moisture content, stable medicament quality and full appearance.
US20110184067 O-desmethylvenlafaxine succinate polymorph & process for preparing thereof This disclosure relates to a crystalline form of O-desmethylvenlafaxine and a process for its preparation. The disclosed crystalline form of O-desmethylvenlafaxine can be used for the manufacture of pharmaceutical compositions for the treatment of depression.
CN103705769A Epidemic encephalitis B treatment medicine and preparation method thereof The invention discloses an epidemic encephalitis B treatment medicine and a preparation method thereof. The medicine is prepared by mainly using fermented soybean, olive, Diverse Wormwood Herb, Luffa Vegetable Sponge, Plastrum testudinis, water chestnut, Hedyotis diffusa, Herba Schizonepetae, Rhizoma Phragmitis, magnet and the like according to a certain weight ratio. The medicine has wind dispelling, qi rectifying, heat clearing and detoxifying functions, can be used for treating the epidemic encephalitis B, and has the advantages of fast effectiveness, good curative effect, no toxic side effects, and no recurrence after curing.
CN1733075A Tinea treating drug Disclosed is a tinea-treating drug which is prepared from dexamethasone, camphor, menthol, sulfur flour and myrrh. The medicament has no toxic and side effects to human body.
CN102204910A Pharmaceutical composition of moxifloxacin hydrochloride, and preparation method thereof The invention provides a pharmaceutical composition of moxifloxacin hydrochloride, and a preparation method thereof. The composition mainly comprises moxifloxacin hydrochloride, a melting agent polyethylene glycol 6000 and other excipients. The preparation method mainly comprises the steps of: preparing drug particles by a hot melt granulating technology, and then tabletting or encapsulating.
US7304047 Method of treating substance abuse with quetiapine This invention relates to a method of treating Substance Use such as Substance Abuse or Substance Dependence and in particular to the use of quetiapine in treating such disorders.
WO2013152654A1 Process for preparation of benzylbenzene sodium-dependent glucose cotransporter 2 (sglt2) inhibitors Provided are methods of making compounds having an inhibitory effect on sodium-dependent glucose cotransporter (SGLT) and synthetic intermediates useful for preparing such compounds.
CN102451154A Netilmicin sulfate injection and preparation method thereof The invention relates to a netilmicin sulfate injection and a preparation method thereof. The netilmicin sulfate injection is characterized in that: every 1,000 ml of injection contains 50,000,000 units of netilmicin sulfate, 0.5-2g of an antioxidant and 0.1-1g of a complexing agent, and the pH value of the netilmicin sulfate injection is 5.3-5.7. A preparation process of the netilmicin sulfate injection comprises the following steps of: cooling an appropriate amount of water for injection to below 30 DEG C under the condition that the air cleanliness is in a hundred level; introducing nitrogen to remove oxygen; adding a prescription dose of the antioxidant and the complexing agent into the water for injection for completely dissolving; adding a prescription dose of the netilmicin sulfate into a solution; stirring for completely dissolving; adsorbing with 0.05-0.2 percent (g/ml) needle active carbon; primarily filtering with one set of 1mum filter for removing carbon; adjusting the pH to 5.3-5.7 with a sodium citrate solution; stirring uniformly; fixing the volume to a full dose by using the water for injection; finely filtering with one set of 0.22/0.22mum polypropylene foldable filter core filter and two sets of 0.22/0.22mum polyether sulfone microporous membrane filter core filters for removing bacteria; embedding under a hundred-level condition (introducing nitrogen in the entire process); assisting in sterilizing at the temperature of 100 DEG C; and performing lamp inspection and packaging. Due to the adoption of a scientific formula and process, the stability of the netilmicin sulfate injection is ensured; and due to the adoption of a sterile assistant sterilization preparation method, the sterile guarantee level of a medicament is raised.
EP2560488A1 Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use Provided are compounds of Formula I: Formula I or a pharmaceutically acceptable salt thereof, wherein R2, R4, R5, R6, R7, R8, R9, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
US20080063654 Prostate Cancer Vaccine Androgen receptor-based vaccines for eliciting an immune reaction in vivo against cells expressing androgen receptor are disclosed. The vaccines are useful in the treatment of prostate cancer. Also disclosed are methods for inducing immune reaction to androgen receptor or treating prostate cancer in a mammal, using the vaccines and pharmaceutical compositions comprising the vaccines.
EP0910564B1 D-amino acid derived inhibitors of cysteine and serine proteases The present invention is directed to novel (D)-amino acid containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
WO2003070910A3 INHIBITION OF VASCULAR ENDOTHELIAL GROWTH FACTOR (VEGF) AND VEGF RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) The present invention concerns methods and reagents useful in modulating vascular endothelial growth factor (VEGF, VEGF-B, VEGF-C, VEGF-D) and/or vascular endothelial growth factor receptor (e.g., VEGFr1, VEGFr2, and/or VEGFr3) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against VEGF and/or VEGFr gene expression and/or activity. The small nucleic acid molecules are useful in the diagnosis and treatment of cancer, proliferative diseases, and any other disease or condition that responds to modulation of VEGF and/or VEGFr expression or activity.
US20080220090 Anti tumor compositions and methods of use An anti-cancer composition having biocompatible materials, which can selectively exploit chemical variations between normal cells and cancer cells to inhibit or prevent the proliferation of cancerous cells and methods of use.
CA2321687C Combination of a selective nmda nr2b antagonist and a cox-2 inhibitor The present invention provides a combination of a selective NMDA NR2B antagonist and a COX-2 inhibitor for the treatment or prevention of pain or nociception.
WO2012162627A1 Treatment of angiogenic- or vascular-associated diseases Described herein are methods and compositions comprising a compound of formula (I), e.g., dehydro-alpha-lapachone, or an analog, derivative, isomer, prodrug, or pharmaceutically acceptable salt thereof, for treatment and/or prevention of angiogenic- or vascular-associated diseases or disorders. The compound has anti-vascular activity. In some embodiments, the compound has anti-vascular activity that targets pathways other than VEGF pathways. In some embodiments, the compound or the composition further comprises anti-tumor activity. In some embodiments, the compound or the composition can decrease adhesion or motility of at least one cell (e.g., endothelial cells or cancer cells).
CA2493483C Endiandric acid h as c-maf inhibitors derivatives for use against asthma The invention relates to compounds of formula (I), to methods for the production thereof from the plant Beilschmiedia fulva, PLA 101037, and to the use of the same for producing a medicament which is especially used to treat allergic illnesses, asthmatic illnesses, and inflammatory concomitant symptoms of asthma and/or of illnesses which can be treated by inhibiting c-maf and NFAT.
CN1883454A Liposome administration system with tumor necrosis targeted antibody for preposition and application thereof The invention discloses a biotinylated tumor necrosis targeting single-chain antibody pre-positioning liposome administration system and the use in tumor treatment, wherein the liposome administration system comprises biotinylated tumor necrosis targeting single-chain antibody and PEG end covalence coupled streptavidin or space stabilized liposome of the streptavidin.
EP1658860A1 Drug compositions comprising anticholinergics and EGFR kinase inhibitors A medicament (A) comprises a combination of 6beta ,7beta -epoxy-3beta -hydroxy-8-methyl-1alpha H,5alpha -H-tropanium salt 2,2-diphenylpropionate ester anticholinergic agent(s) (I) and EFGR kinase inhibitor(s) (II), optionally together with auxiliaries. A medicament (A) comprises a combination of tropane derivative anticholinergic agent(s) of formula (I) and EGFR kinase inhibitor(s) (II) (optionally in the form of enantiomers, enantiomer mixtures or racemates, or solvates or hydrates), optionally together with pharmaceutical auxiliaries. [Image] X->monovalent anion, preferably chloride, bromide, iodide, sulfate, phosphate, methanesulfonate, nitrate, maleate, acetate, citrate, fumarate, tartrate, oxalate, succinate, benzoate or p-toluenesulfonate. An independent claim is also included for new anticholinergic agent(s) of formula (I). - ACTIVITY : Antiinflammatory; Antiasthmatic; Antiallergic; Hypotensive. No biological data available. - MECHANISM OF ACTION : Anticholinergic; EFGR kinase inhibitor.
US20110200527 Peptide Ligand Directed Drug Delivery Provided is a novel peptide ligand (Leu-Ala-Arg-Leu-Leu-Thr) for binding to an EGFR surface pocket based on its 3D crystal structure. When conjugated to the distal end of liposome surface PEG moieties, the peptide ligand directs liposome binding and uptake by EGFR high expressing cancer cells (H1299 and SPCA1) specifically and efficiently. The targeted delivery of liposomal anticancer drug doxorubicin results in better therapeutic efficacy towards cells in vitro. In vivo, the targeted liposomes are injected via tail vein and the time course of their distribution and accumulation in xenograft tumor tissues are studied using a live animal fluorescence imaging system. The LARLLT targeted liposomes were seen to gradually concentrate at the tumor site and be preferentially retained more than 80 hours after injection.
US20060148908 Supressant of toxicity induced by cancer chemotherapeutic agent and composition of cancer chemotherapeutic agent containing the same Disclosed are a suppressant of toxicity such as hepatotoxicity and nephrotoxicity, induced by cancer chemotherapeutic agent, and a composition of cancer chemotherapeutic agent containing the suppressant. The suppressant of toxicity induced by a cancer chemotherapeutic agent contains xanthorrhizol as an active ingredient. Xanthorrhizol shows an excellent ability in suppressing ill effects generated by dosage of cancer chemotherapeutic agent, such as hepatotoxicity and nephrotoxicity.
US20090123425 Macrocyclic, pyridazinone-containing hepatitis c serine protease inhibitors The present invention relates to compounds of Formula I, II, or III, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.
WO2008124000A3 Thiazole derivatives as androgen receptor modulator compounds Provided herein are compounds of formula (I), (II), (III) or (IV) that bind to androgen receptors and/or modulate activity of androgen receptors and/or modulate the amount of androgen receptors and/or reduce the number of androgen receptors in a cell and/or degrade androgen receptors in a cell; and to methods for making and using such compounds. Also provided are compositions containing such compounds and methods for making and using such compositions.
US20130030034 Modulation of timp1 and timp2 expression Provided herein are compositions, methods and kits for modulating expression of target genes, particularly of tissue inhibitor of metalloproteinase 1 and of tissue inhibitor of metalloproteinase 2 (TIMP1 and TIMP2, respectively). The compositions, methods and kits may include nucleic acid molecules (for example, short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA) or short hairpin RNA (shRNA)) that modulate a gene encoding TIMP1 and TIMP2, for example, the gene encoding human TIMP1 and TIMP2. The composition and methods disclosed herein may also be used in treating conditions and disorders associated with TIMP1 and TIMP2 including fibrotic diseases and disorders including liver fibrosis, pulmonary fibrosis, peritoneal fibrosis and kidney fibrosis.
CN102643316A Acylated glycoside compounds as well as production method and application thereof The invention provides acylated glycoside compounds as well as a production method and application thereof. The acylated glycoside compounds are characterized by comprising the following structural general formula: R1 is H, OH or OAc and R2 is toluenesulfonyl group and salicyl. The acylated glycoside compounds disclosed by the invention have an immune regulation function and can be used for preparing medicaments for treating rheumatoid arthritis, medicaments for treating autoimmune diseases such as systemic lupus erythematosus, eczema and parapsoriasis guttata as well as medicaments for treating various immunological diseases such as allergic reaction.
CN103130815A Isosorbide mononitrate derivative and preparation method and application thereof The invention discloses an isosorbide mononitrate derivative, a preparation method thereof and an application thereof to tumor combined treatment as shown in the formula (II). Ester is formed by isosorbide mononitrate and fatty acid through an esterification reaction, so that lipid solubility can be improved, and then a lipid nanoparticle passive targeting drug delivery system is further prepared. Afterwards, the drug combination is conducted by lipid nanoparticles of an isosorbide mononitrate fatty acid derivative and nano targeting anticancer drugs, and the therapeutic effect of chemotherapeutic drugs is improved.
US20120136022 Gastric retentive extended-release dosage forms comprising combinations of a non-opioid analgesic and an opioid analgesic Compositions and methods for the treatment of pain in a mammal are described. More specifically, a dosage form designed for release of acetaminophen and an opioid is described, wherein the dosage form provides delivery of the drugs to the upper gastrointestinal tract (“GI”) of a mammal for an extended period of time.
WO2014070991A3 Galactopyranosyl-cyclohexyl derivatives as e-selectin antagonists Provided herein are E-selectin antagonist therapeutic agents and improvements thereto and compositions comprising these E-selectin antagonists. Methods are also provided for using these E-selectin antagonist therapeutic agents to treat and/or prevent diseases and disorders treatable by inhibiting binding of an E-selectin to an E-selectin ligand. Also provided herein improvements to E-selectin antagonist giycomimetic compounds that improve the oral bioavailability of the giycomimetic compounds.
US20120022079 Method For Producing Preparations Of Substances Poorly Soluble In Water The invention relates to a process for producing formulations of sparingly water-soluble substances, said sparingly soluble substances being present in amorphous embedded form in a copolymer, and said copolymer being obtained by free-radically initiated polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the sum of components i), ii) and iii) equals 100% by weight, which comprises embedding the sparingly soluble substance into the copolymer at temperatures above the melting point of the sparingly soluble substances.
US7229974 Used to diagnose or treat cancer, restenosis, a disease caused by a virus, a disease affected by integrins or cell-cell adhesion receptor or a disease triggered by diffusible factors Oligonucleotides of the formula 5′-(CAP)-(Oligo)-(CAP)-3′ are disclosed where (oligo) is a nucleotide sequence of from 10 to 40 nucleotides in length, and CAP is Gm, where m is an integer of from zero to ten, the two CAP's which are present in the molecule can be defined independently of each other and must be different in the case where m is zero at the 5′ or 3′ end and the end of the Oligo sequence is other than guanine. The oligonucleotides can be synthesized chemically. The oligonucleotides are used to diagnose or treat cancer, restenosis, a disease caused by a virus, a disease affected by integrins or cell-cell adhesion receptor or a disease triggered by diffusible factors.
WO2010080769A3 Chemotherapeutic methods and compositions Disclosed herein are methods and compositions for enhancing the cell-killing activity of anti-neoplastic agents by inhibiting the activity of a lysyl oxidase-type enzyme. Also disclosed are methods for screening for chemotherapeutic agents, and for molecules that enhance the activity of chemotherapeutic agents, using cells grown on an extracellular matrix.
CN102100685A PTP1B inhibitor and synthetic method and application thereof The invention relates to a chemical total synthesis method of a novel PTP1B inhibitor and an application in drugs for treating type 2 diabetes mellitus. The chemical structural formula of the PTP1B inhibitor is as follows, wherein each carbon at 2, 2', and 3' position of a phenyl ring is connected with a bromine atom; each carbon at 4, 4', 5, 5' position is connected with a hydroxyl; the chemicalname in English is (2'-bromo-4',5'-dimethoxy-phenyl)-(2,3-dibromo-4,5-dihydroxy-phenyl)-methanone. The compound enhances the sensitivity of insulin receptors by inhibiting the activity of protein tyrosine phosphatase 1B, and has a good therapeutic effect on insulin resistant type 2 diabetes mellitus.
EP2396034A1 Antibodies and methods for treating estrogen receptor-associated diseases Provided herein in certain embodiments are antibodies, antibody fragments, pharmaceutical compositions, methods for modulating the functions of estrogen receptor alpha 36, and methods for preventing and/or treating diseases mediated by estrogen receptor alpha 36.
CN1618427A Medicinal resin biological adhering slow-releasing liquid prepn. contg. aciclovir, and its prepn. method A slow-release antiviral medicine in the form of liquid is prepared from acyclovir (30-90 wt%) and auxiliary (10-70 wt.%) including the cationic exchange resin and ethylcellulose and/or acrylic resin for slow releasing and the hydroxypropyl cellulose for adhering. Its advantages are high curative effect and low toxic by-effect.
CN1951938A Penehyclidine quaternary ammonium salt and its derivative The invention discloses an ethyl ether quaternary ammonium salt and derivant as Choline-proof compound and preparing method with the following structure, wherein R is C1-C6 paraffin or substituted phenyl C1-C6 paraffin, which is methyl, phenylmethyl, ethyl group, propyl or isopropyl at best; M is halogen, which is F, Cl, Br or I at best. The invention can treat peripheral cholinergic nerve from exciting.
WO2010045276A3 Azabenzimidazolones Compounds are provided having the general structure of formula I: In formula I, one member of the group (W, X, Y and Z) is a nitrogen atom and the remaining three members of the group are each independently a carbon atom covalently bonded to a radical, R4. The radicals, R1 R2, R3 and R4 are each defined herein, and n is an integer from 1 to 4. Also provided are stereoisomers, prodrugs, pharmaceutically acceptable salts, hydrates, salt hydrates, acid salt hydrates, and polymorphs of the compounds having the structure of formula I. The compounds bind the prostaglandin D2 receptor and are useful in the prophylaxis and treatment of prostaglandin D2-mediated diseases and conditions, including pain and inflammation, as well as asthma and allergic diseases and conditions.
WO2013168023A1 Compositions and methods for treatment of parkinson's disease Provided are compounds, pharmaceutical acceptable salts, polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising the compounds may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral admimstration, syrup or injection, and may be used for the treatment of Parkinson's disease, Huntington's disease, Alzheimer's disease multiple sclerosis lateral sclerosis and neural motor disorders.
CN101138567A Natural glycosides component having good effect of reducing blood sugar The invention discloses a natural small-molecule glycoside compound of better hypoglycemic activity, which is selected from the natural similar compounds through screening test. The invention provides a better choice for the development of the compound and the new drug in clinically treating diabetes.
WO2012091115A1 Acetylene derivative and pharmaceutical application therefor A novel compound with a uric acid generation inhibiting action is provided. The present invention pertains to an acetylene derivative indicated in formula (I), a prodrug thereof, or a salt of same, that has a xanthine oxidase inhibitory activity and is useful as a prophylactic or therapeutic agent for diseases caused by an abnormal serum urate level. In formula (I): R1 is a hydrogen atom, a C1-6 alkyl, or a C3-8 cycloalkyl, etc.; M is a C6-10 aryl or 5- or 6-membered cyclic heteroaryl; Q is carboxy, etc.; Y independently represents a hydroxyl group or a C1-12 alkyl, etc.; and n is 1 or 2. The group represented by -W-M is a group etc., represented by formula (A), wherein: T is cyano, etc.; and R2 is a hydrogen atom, a fluorine atom, a C1-6 alkyl, or a C1-6 alkoxy, etc.
US7858659 Redox therapy for tumors The invention provides methods and compositions for treatment of tumors comprising administering to subject bearing a tumor an effective amount of at least one agent that decreases the [GSH]2/[GSSG] ratio in the malignant cells of said tumor, wherein said at least one agent is administered continuously to said patient for a period of time within the range of from about 15 to about 75 hours.
CN102772425A Anti-pulmonary fibrosis application of small interfering RNA of Fstl 1 The invention discloses an application of small interfering RNA of Fstl 1 in anti-pulmonary fibrosis. Pharmacology experiments confirm that the small interfering RNA of Fstl 1 can effectively reduce a mortality rate of bleomycin-instilled mice, and pulmonary damage and pulmonary fibrosis which are induced by bleomycin can be reduced significantly via decreasing expression of Fstl 1, thereby indicating that the small interfering RNA of Fstl 1 can be used for preparing drugs for preventing and/or treating pulmonary fibrosis.
CN102361639A Adhesive patch-containing package bag and method for storing adhesive patch Disclosed is an adhesive patch-containing package bag (1) which comprises a package bag (8) and an adhesive patch (10) enclosed within the package bag (8), characterized in that: the adhesive patch (10) comprises a support (12), a pressure-sensitive adhesive layer (14) being superposed on at least one side of the support (12) and containing ropinirole and/or a pharmaceutically acceptable salt thereof, and a release film (16) covering the pressure-sensitive adhesive layer (14); and the relative humidity at 4oC in the interior of the package bag (8) is maintained at 35% or higher.
CN101391061A Novel antibiotic substitute The invention discloses a preparation for novel antibiotic substitute and a preparing art and mainly relates to the agricultural biotechnology and feed additive field. The preparation includes montmorillonite gel, sodium metasilicate, carbonate, reducing sugar, sodium selenite and rice bran. Adopting the solid aerobic biological fermentation, the preparation has simple art and fine stability. The preparation can improve animal healthy level and the resistance ability and anti-stress capability for pathogeny microbial beings through enhancing animal nonspecific and specific immunity ability, so as to improve animals food consumption, daily gain and food conversion ratio, ensure animals producing performance under the no antibiotic condition, and avoid the generation of antibiotic remain and drug-resistant strain in the animals production. The preparation can play an important role in improving the stockbreeding sustainable development and enhancing human healthy level.
WO2008096779A1 C70-containing liposome, method for producing the same, and use of the same A solution containing a cyclodextrin-C70 complex is mixed with a solution containing a liposome-forming lipid at 10-45˚C, thereby producing a C70-containing liposome having the intrinsic physical properties of C70 fullerene, which liposome is stably soluble in a polar solvent. Specifically disclosed are a C70-containing liposome which has the intrinsic physical properties of C70 fullerene and is stably soluble in a polar solvent, a method for producing such a C70-containing liposome, and a use of such a C70-containing liposome.
EP1542681A2 Use of posaconazole for the treatment of fungal infections The use of posaconazole for the preparation of a medicament for the treatment or prevention of fungal infections in humans of 12 years and older in need of such treatment or prevention the medicament which comprises an effective amount of posaconazole in divided doses two to four times a day to produce an arithmetic mean steady state average maximum plasma concentration of posaconazole of at least about 300 ng/mL to at least about 550 ng/mL is disclosed.
CN101757382A Plaster for accelerating Hepatitis B curing The invention relates to a plaster for accelerating hepatitis B curing, which is an externally applied product invented at present for specially treating hepatitis B. A hepatitis B disease is an infectious disease which is caused by hepatitis B viruses, takes hepatic lesion and hepatic necrosis lesion as main forms, has high infectivity, wide prevalent scope and high morbidity and is the most terrible disease which is most difficult to cure. Before the hepatitis B enzyme-reducing pill, no excellent Chinese patent medicine preparation is discovered to cure the hepatitis B in the market; and the invention belongs to pure Chinese patent medicine preparations and has an excellent curative effect on the hepatitis B disease.
US20100056516 1-hydroxy naphthyridine compounds as anti-hiv agents 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.
WO2012041934A1 Polysubstituted 2-aminoimidazoles for controlling biofilms and process for their production The present invention relates to compounds, compositions and methods for controlling and/or preventing biofilms and bacterial infections, being polysubstituted 2-amino-imidazoles with the structural formula (I). wherein R1 is H, an aliphatic group or a cycloaliphatic group; R2 is H, an aliphatic group or a cycloaliphatic group; R3 is an aliphatic group, a cycloaliphatic group, an aromatic group or a heterocyclic group; and R4 is an aliphatic group, a cycloaliphatic group, an aromatic group or a heterocyclic group; and pharmaceutically acceptable salts, hydrates, solvates, prodrugs, stereoisomeric forms or polymorphic substances thereof.
US20080070972 for an oral cytokine inhibitor of interleukin-1 beta converting enzyme; antiinflammatory agent: rheumatoid arthritis and psoriasis; wet granulated compound with the organic solvent, a first and second binding agent, porous agent, glidant, lubricant The invention relates to a controlled release formulation for an oral cytokine inhibitor of interleukin-1 beta converting enzyme.
CN103232509A Fluorouracil compound, and preparation method and application thereof The invention discloses series of compounds of fluorouracil in 1- or 3-triazole rings and a preparation method of compounds, belongs to the field of medicinal chemistry, and particularly relates to a novel fluorouracil antitumor compound with the following general formula of chemical structure. The fluorouracil compound has antitumor activity; and the preparation method is economical, simple, mild and efficient.
WO2010068717A2 Pyrazolinone scavengers of free radicals The present invention relates to new pyrazolinone scavengers of free radicals, pharmaceutical compositions thereof, and methods of use thereof.
EP1633733B1 Cannabinoid derivatives, methods of making, and use thereof 1'-substituted cannabinoid derivatives of delta-8-tetrahydrocannabinol, delta-9-tetrahydrocannabinol, and delta-6a-10a-tetrahydrocannabinol that have affinity for the cannabinoid receptor type-1 (CB-1) and/or cannabinoid receptor type2 (CB-2). Compounds having activity as either agonists or antagonists of the CB-1 and/or CB-2 receptors can be used for treating CB-1 or CB-2 mediated conditions.
WO2013051632A1 Nitrogen-containing fused heterocyclic compound The present invention provides a novel compound which has excellent activity as an ERRα modulator and is useful as a therapeutic or prophylactic agent for ERRα-related diseases such as cancers, or the like. The present invention relates to a compound represented by formula (I) or a salt thereof. (In formula (I), A represents an optionally substituted cyclic group; La represents a bonding hand or the like; Lb represents a C1-3 alkylene group or the like; Lc represents a bonding hand or the like; G represents a group represented by formula Ga or Gb (wherein each of Z1, Z2, Z3 and Z4 independently represents a nitrogen atom, a carbon atom, -CH- or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like); and E represents a group represented by formula Ea or Eb (wherein X represents -S- or the like; and each of R1, R2 and R3 independently represents a hydrogen atom or the like).)
WO2012101063A1 N-acyl pyridine biaryl compounds and their uses The present invention provides a compound of general formula:wherein Z2-Z6 include one or two nitrogen atoms as described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
US20100179164 2,4-pyrimidinediamine compounds for treatment of inflammatory disorders 2,4-Pyrimidinediamine compounds represented by formula (I), methods for preparing the same and methods for treating an inflammatory disorder and for inhibiting the production of IL-23 and/or stimulating the production of IL-10 using the same:
US20080293788 Methods and Compositions for the Treatment of Pulmonary Diseases This invention related to methods of treating, preventing and managing various pulmonary diseases or disorders using formoterol in combination with calcium activated potassium channel openers. Pharmaceutical compositions comprising formoterol and calcium activated potassium channel openers are also disclosed.
WO2005032543A1 Hypnotic composition [PROBLEMS] To provide a hypnotic composition in which side effects of an antihistaminic agent on the central nervous system (unpleasant feeling after awakening and boredom) have been reduced without adversely influencing the hypnotic activity of the antihistaminic agent. [MEANS FOR SOLVING PROBLEMS] Vitamin E or an analogue thereof is used in combination with an antihistaminic agent having hypnotic activity, preferably at least one member selected from the group consisting of ethanolamine compounds, propylamine compounds, phenothiazine compounds, piperazine compounds, piperidine compounds, and pharmaceutically acceptable salts of these.
WO2013191158A1 Percutaneous absorption promoter and skin patch comprising same A percutaneous absorption promoter for promoting percutaneous absorption of diclofenac sodium, the promoter containing 1-menthyl glyceryl ether and a petroleum-based resin and/or terpene-based resin; and a skin patch comprising the same.
WO2006137106A3 Method for the potentiation of opioid analgesics effects on pain According to the invention there is provided use of an anti-TrkA antibody capable of inhibiting the binding between NGF and TrkA combined with at least one opioid analgesic for the preparation of a medicament for treating and/or preventing pain.
CN101559207A Chinese patent medicine for treating cervical spondylosis The invention belongs to a Chinese patent medicine for treating cervical spondylosis, which is prepared from medicines comprising angelica dahurica, myrrh, achyranthes, rhizoma ligustici wallichii, frankincense, cassia twig, hurricane lamp, Clematis chinensis, ginger, Gentiana macrophylla, angelica, notopterygium root, and the like. The Chinese patent medicine has no side effect, directly acts on pain points, treats both the principal and the secondary aspect of a disease and has obvious effect.
US20120258945 Association Between Ferroquine and an Artemisinine Derivative for Treating Malaria This invention is directed to methods for the treatment and prevention of malaria comprising administering a combination of ferroquine, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and an artemisinin derivative, and to pharmaceutical compositions comprising such combination.
CN101507818A Capsaicin beta-cyclodectrin inclusion-compound and liposome and gel of inclusion-compound The invention discloses a capsaicin beta-cyclodextrin inclusion compound, as well as liposome and gel thereof. The capsaicin beta-cyclodextrin inclusion compound is prepared by the following method: (1) beta-cyclodextrin is dissolved in an aqueous phase and prepared into a solution, and the solution is added with capsaicin or a capsaicin solution so as to obtain a mixed solution of capsaicin and beta-cyclodextrin; and (2) the solution-type capsaicin beta-cyclodextrin inclusion compound is obtained from the mixed solution prepared in a step (1) through at least one treatment mode of standing, heating, stirring, ultrasound or grinding. The apparent solubility of the capsaicin of the inclusion compound increases by 2 to 20 times. In vitro transdermal study shows that the capsaicin inclusion compound can obviously raise the transdermal rate of medicine by 5 to 20 times as compared with cream and hydrogel, and obviously reduce the irritation of capsaicin at skin. Besides transdermal drug administration, the prepared inclusion compound and the inclusion compound liposome can also be orally taken, injected or administrated in bladders. In addition, the invention is simple in production process, and the quality is stable and easy to control.
WO2009119667A1 Helicobacter pylori GROWTH INHIBITOR AND METHOD FOR PRODUCTION THEREOF Disclosed is an inhibitor of the growth of Helicobacter pylori, which comprises a culture supernatant of a plant-derived lactic acid bacterium having 16S rRNA comprising a nucleotide sequence depicted in any one of SEQ ID NO:1 to SEQ ID NO:4 or an extract from the culture supernatant. It becomes possible to provide a novel technique for inhibiting the growth of Helicobacter pylori without supplying living cells of Helicobacter pylori to the stomach.
US7678787 Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2).
WO2014113467A1 Stat3 inhibitor Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.
US6887875 2,5-diarypyrimidine compounds Diarylpyrimidine compounds of Formula I are provided, wherein. or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are independently chosen from: phenyl which is mono-, di-, or tri-substituted, 1-naphthyl and 2-naphthyl, each of which is optionally mono-, di-, or tri-substituted, and optionally mono-, di-, or tri-substituted heteroaryl, said heteroaryl having from 1 to 3 rings, 5 to 7 ring members in each ring and, in at least one of said rings, from 1 to about 3 heteroatoms selected from the group consisting of N, O, and S; R is oxygen or absent; Z2 is CR2; Z3 is nitrogen; R1 and R2 are independently chosen from hydrogen, halogen, amino, cyano, nitro, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted mono- or di-alkylamino, optionally substituted cycloalkyl, optionally substituted (cycloalkyl)alkyl, optionally substituted (cycloalkyl)oxy, optionally substituted (cycloalkyl)alkoxy, optionally substituted alkylthio, optionally substituted alkylsulfinyl, optionally substituted alkylsulfonyl, and optionally substituted mono- or dialkylcarboxamide; with the proviso that not all of R1, R3, and R4 are hydrogen. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatments of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of Formula I are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
WO2013027895A1 Composition for inhibiting angiogenesis containing a peroxidasin inhibitor as an active ingredient The present invention relates to a composition for inhibiting angiogenesis containing a peroxidasin inhibitor as an active ingredient. More particularly, the present invention relates to a method for screening for an angiogenesis inhibitor, comprising the steps of: treating a test material and a pharmaceutical composition for inhibiting angiogenesis containing a peroxidasin gene expression inhibitor as an active ingredient or an activation inhibitor of a peroxidasin protein, and then analyzing the expression of the peroxidasin gene or the activity of the protein; and comparing the gene expression or protein activity of peroxidasin, which has not been treated with the test material, with that of peroxidasin which has been treated with the test material. Therefore, the inhibitor according to the present invention, which inhibits the expression of peroxidasin or the protein activity, can effectively inhibit cell migration, cell proliferation, and vasculogenesis in endotheliocytes and can thus be valuably used to effectively prevent or treat various diseases or conditions mediated by abnormal angiogenesis.
EP2499112A1 Substituted 3-(phenoxymethyl) benzyl amines and personal care compositions Certain novel substituted 3-(phenoxymethyl) benzyl amines and personal care compositions comprising such, which are particularly beneficial for skin lightening and achieving evenness of color, especially for face and underarm skin.
WO2006084934A1 Use of thiadiazolidine-derived compounds as neurogenic agents The invention relates to the use of heterocyclic compounds in the preparation of a medicament for regenerating damaged neuronal tissue. In a preferred embodiment of the invention, compounds having formula I are used to produce a medicament for the regeneration of neuronal tissue in pathologies or conditions involving neuronal damage or death in the central nervous system or in the peripheral nervous system.
US7820713 Cocoa extracts as antioxidants Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topoisomerase-inhibiting compositions and methods.
WO2008007131A2 Treatment for demyelinating disease The invention relates to a method of treatment or prophylaxis of demyelinating disease, in particular the neurodegenerative phase of demyelinating disease, which comprises administration of an acid sensing ion channel (ASIC) antagonist. The invention also relates to a pharmaceutical composition comprising an ASIC antagonist in combination with an additional therapeutic agent, in particular an anti-inflammatory or immunmodulatory agent.
EP1276460B1 Use of preparations containing an extract of the plant argania spinosa in cosmetic care products for hair and skin The invention relates to cosmetic and/or pharmaceutical preparations that contain saponins derived from an extract of the plant Argania spinosa.
EP2436379A1 Stable tablet formulation The present invention is directed to a stable solid formulations of tetrahydrobiopterin, processes for producing them, and treatment methods using such formulations.
WO2009146696A1 Use of indole-3-carboxylic esters for inhibiting microsomal prostaglandin e2 synthase The present invention relates to the use of indole-3-carboxylic esters and derivatives thereof for inhibiting inducible microsomal prostaglandin E2 synthase-1 and/or for inhibiting 5-lipoxygenase. More particularly, the invention relates to the use of derivatives of 3‑carboxyaryl[g]indole, in particular of 2-aryl- and 2-arylalkylaryl[g]indole-3-carboxylic esters and structural derivatives thereof for inhibiting inducible microsomal prostaglandin E2 synthase-1 and/or for inhibiting 5-lipoxygenase. The invention further relates to the use of indole-3-carboxylic esters for producing a medicament for treatment of PGE2- and/or 5-LO-mediated disorders and pathological states, especially of inflammatory chronic inflammations such as rheumatoid arthritis, osteoarthritis, disorders of the cardiovascular system, asthma, allergic rhinitis, multiple sclerosis, inflammatory skin disorders, osteoporosis and cancer, pain and fever, in which PGE2 and/or 5-LO products are involved.
US20110081297 Novel Substituted Pyrazoles, 1,2,4-Oxadiazoles, and 1,3,4-Oxadiazoles The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted pyrazole derivatives, compositions, and therapeutic uses and processes for making such compounds.
US20100074958 Methods and compositions for targeting fenestrated vasculature Targeting of a fenestrated vasculature at a body site by micro or nanoparticles can be increased by using particles that have a radius substantially equal to a critical radius of a normal vasculature at the body site. The particles can be used for treating or monitoring a physiological condition responsible for the fenestrated vasculature. A method of improving an ability of micro or nanoparticles to target fenestrated blood vessels in a body site by selecting particles from a population of the micro or nanoparticles, where the selected particles have a radius that permits enhanced delivery into the fenestrated blood vessels.
CN102612365A Checkpoint kinase 1 inhibitors for potentiating DNA damaging agents A CHK1 inhibitor for administration to a patient with cancer for potentiating a DNA damaging agent is provided.
CN103285239A Traumatic The invention discloses traumatic which is prepared from the following medicinal raw materials by weight: 0-30g of rosin, 0-25g of daemonorops draco, 0-20g of bletilla striata, 0-20g of golden cypress, 0-30g of Yunnan pseudo-ginseng, 0-10g of centipede, 0-10g of pearl, 0-15g of crinis ustus, and 0-25g of gypsum. The traumatic has a significant treatment effect.
CN102949408A Pharmaceutical composition capable of strengthening immunity of poultry and method for preparing pharmaceutical composition The invention provides a pharmaceutical composition capable of strengthening the immunity of poultry. The pharmaceutical composition comprises, by weight, from 5 to 15 parts of butafosfan, from 1 to 10 parts of astragalus polysaccharide and the balance adjuvant materials, and the astragalus polysaccharide is extracted by a method including steps of water boiling backflow and ethanol precipitation. By the pharmaceutical composition, both a cellular immunity level and a humoral immunity level of a poultry organism are obviously improved, particularly, the cellular-level immunity of the poultry organism is strengthened, and accordingly the integral immunity of the poultry organism is effectively strengthened. In addition, by using the pharmaceutical composition with a vaccine, avian antibody titer can be increased, the quantity of generated antibodies is high, the antibodies can be maintained for a long time, and an immunopotentiation effect is obvious. Accordingly, the pharmaceutical composition can be used for cooperative medication for avian Newcastle diseases, bursa of Fabricius, avian influenza and the like, antibody protection time is prolonged, the usage and the usage count of vaccines are reduced, and prevention and treatment effects of the vaccines are improved. The pharmaceutical composition can be used for preventing sudden and serious avian diseases, and accordingly prevalence of common avian diseases is avoided.
CN101525336B Carbapenem compound containing substituted formohydrazide group The invention belongs to the field of medical technologies, and more particularly relates to a carbapenem compound containing a substituted formohydrazide group as shown in the general formula (I), and pharmaceutically acceptable salt, easily-hydrolytic ester, isomer, hydrate and the hydrates of the ester or the salt thereof, wherein R<1>, R<2>, R<3>, R<4>, R<5> and R<6> are as defined in the specification. The invention also relates to a preparation method of the compound, pharmaceutical composition containing the compound, and the application of the compound in preparing a drug for treatingor preventing infectious diseases.
EP1222265B1 Novel nicotinic acetylcholine receptor subunit, its isolation and use HNARA10 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. HNARA10 polypeptides belong to the family of nicotinic acetylcholine receptors. Also disclosed are methods for utilizing HNARA10 polypeptides, polynucleotides and antibodies in the design of protocols for the treatment of various diseases, among others and diagnostic assays for such conditions.
CA2250318C Sustained-release metal valproate tablets The present invention provides a sustained-release metal valproate tablet which is comparatively compact and is not influenced by a meal, the sustained-release metal valproate comprising a core tablet comprising a metal valproate having on the surface a coating layer comprising light silicic acid anhydride dispersed in a mixture of ethyl cellulose and a methacrylic acid-methyl methacrylate copolymer.
CN1853618A Use of bromphenol compound in protein-tyrosine phosphonatease inhibitor An application of the bromophenol compounds chosen from bis-(2,3-bibromo-4,5- dihydroxybenzyl)-ether, 2,2',3,3'-tetrabromo-4,4',5,5'-tetrahydroxydiphenyl methane, 2,2',3- tribromo-3',4,4',5-tetrahydroxy-6'-ethoxymethyl diphenylmethane, 3-bromo-4,5-bis-(2,3-dibromo -4,5-dihydroxybenzyl)-catechol, their pharmacologically acceptable derivatives, and their mixture in preparing the depressant of protein tyrosine phosphatase for treating diabetes and obesity is disclosed.
WO2003101425A3 Therapeutic agent-containing polymeric nanoarticles Hydrophilic polymeric articles comprising a polymeric scaffold covalently attached to one or more therapeutic agents, such as drug or drug-conjugate molecules. The articles may further covalently attached comprise recognition elements (REs) that bind to biomolecular structures expressed on certain cells or in certain tissues, to facilitate targeting and/or delivery.
WO2013005170A3 Inhibitors of aquaglyceroporins, methods and uses thereof The present invention discloses metal-based modulators that selectively bind to cell transmembrane proteins aquaglyceroporins AQPs, such as AQP3, AQP7 and AQP9, leading to its inhibition. The selective inhibition of AQP channels is accomplished by compounds tetracoordinated to gold (III) complexes. The present invention also discloses the uses thereof in manufacturing pharmaceuticals, cosmetics and chemical reagents for diagnostic, treatment, prophilaxys and prevention of clinical conditions directly or indirectly related to aquaglyceroporins AQPs functions. The present invention applies in healthcare and cosmetic industries and in chemistry industry.
EP1246841B1 Transcription factors containing two potential dna binding motifs There is disclosed an isolated protein comprising (i) a winged helix motif which has the potential capability of binding to nucleic acid and (ii) a Cys2-His2 zinc finger motif which also has nucleic acid binding capability and nucleic acid molecules encoding therefor.
CN102349868A Preparation method of targeting folic acid-hydrophobic anticancer drug hydrogel The invention relates to a preparation method of small molecular hydrogel precursor molecules based on folic acid-anticancer drugs. The obtained compound is prepared into small molecular hydrogel by reducing disulfide bonds using reducing agents (glutathione and dithiothreitol). Specifically, the preparation method comprises the following steps of: firstly, synthesizing folic acid connected small peptides by a solid phase synthesis method, then derivatizing an anticancer drug (taxol, camptothecin, hydroxycamptothecine and the like) by butanedioic anhydride or glutaric anhydride to remove one carboxyl group, and connecting the folic acid connected small peptides with the derivatized anticancer drug. The precursor molecules not only have a targeting effect, but also have good solubility and are capable of self assembling into small molecular hydrogel by reduction of the disulfide bonds. The novel transmission system of the hydrophobic anticancer drug established by the invention not only greatly improves the solubility of the hydrophobic anticancer drug in water, but also is capable of targeting tumor tissues, thus reducing toxic side effects.
EP2724729A1 Apoptosis-inducing agent This invention relates to: a novel use of GST-π and GST-π suppressing agents; an apoptosis-inducing agent containing as active components a drug that suppresses GST-π and a drug that suppresses autophagy; a medical composition containing said agent; and a method using said medical composition for treating diseases associated with abnormal apoptosis.
WO2010103064A1 Novel benzoxazinone derivatives useful for the treatment of cns disorders The present invention encompasses novel 1,4-dihydro-3,1-benzoxazin-2- one derivatives, which are surprisingly found to be efficacious in animal models of CNS disorders and, as such, are valuable candidates for the prevention or treatment of CNS (Central Nervous System) diseases or disorders.
EP0837681B1 Use of 19-nor-vitamin d compounds for the prevention of hyperphosphatemia in kidney disorder patients The 19-nor-vitamin D analogs, and particularly 19-nor-1 alpha ,25-dihydroxyvitamin D2, possess low calcemic and phosphatemic activity while also having the ability to suppress parathyroid hormone (PTH) production. The suppressive effect on PTH secretion of these 19-nor analogs without significant changes in serum calcium or serum phosphorus make them ideal tools for the treatment of secondary hyperparathyroidism in patients having kidney disorders.
US7597899 Compositions comprising a combination of a free sphingoid base and ceramide and uses thereof The present invention discloses a composition for topical use comprising a free sphingoid base and a ceramide. The compositions of the invention are suitable for application to skin conditions associated with an impaired barrier function, in particular to skin conditions further associated with a deranged regulation of cell growth and differentiation, an inflammatory condition and/or an infectious state.
WO2009064417A2 Compositions for the treatment of gastrointestinal inflammation Provided herein are methods for preventing or alleviating the symptoms of and inflammation associated with inflammatory diseases and conditions of the gastrointestinal tract, for example, those involving the esophagus. Also provided herein are pharmaceutical compositions useful for the methods of the present invention.
CN1972943A New derivatives of 5-aryl-1h-pyrrolo [2, 3b] pyridine-3-carboxamide or 5-aryl-1h-pyrrolo [2, 3b] pyridine-3-carboxylic acid The present invention relates to new compounds of formula I as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
US20120232065 Dihydro-oxazolobenzodiazepinone compounds, a process for there preparation and pharmaceutical compositions containing them Compounds of formula (I): wherein: R1 represents a hydrogen atom or an alkyl group; R2 represents an alkyl group; R3 represents an aryl or heteroaryl group. Medicinal products containing the same which are useful in the treatment or prevention of psychiatric and neurological disorders characterised by cognitive deficits.
US20100285123 Controlled Release Dosage Formulation of Duloxetine The preset invention provides a controlled release dosage form of duloxetine comprising a homogenous core comprised of duloxetine or its pharmaceutically acceptable salts, pharmaceutically acceptable polymeric carrier, solubility enhancer, a hydrophobic component, a hydrodynamic diffusion enhancer, a viscolyzing agent and pharmaceutically acceptable excipients; a entering coat on said core and a barrier layer between said core and the enteric coat.
US6933293 Unit treatment dose and patient package The invention relates to the use of mirtazapine for the preparation of a medicine for a new method of treatment of a sleep disorder in a subject, which treatment comprises the administration of mirtazapine with a unit treatment dose comprising between 0.1 and 5 mg mirtazapine and relates to a patient pack for the treatment of sleep disorders.
EP1765330A2 Pyranoindole derivatives and the use thereof for the treatment of hepatitis c virus infection or disease The invention is directed to novel pyranoindole derivatives and analogs as well as compositions containing the same and to the use thereof for the treatment, prevention or inhibition of viral infections and associated diseases caused by the Hepatitis C virus.
US7005450 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives useful as nitric oxide synthase inhibitors The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
WO2011131102A1 Preparation method of lactone and use thereof Disclosed is a preparation method of a sphaelactone which is prepared form parthenolide sphaelactone as raw material and a suitable acid as catalyst in suitable solvent at suitable reaction temperature and the yield is more than 60%. Also disclosed are uses of the sphaelactone and pharmaceutical composition comprising the sphaelactone and pharmaceutically acceptable carrier in preparation of drugs for treating cancer.
WO2010045787A1 The use of ginsenoside compound k in the manufacture of atherosclerosis medicine Use of ginsenoside K (20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol) of the formula below for preparing medicines for preventing and treating atherosclerosis.
US7022734 Use of a transition metal complex, other than deferoxamine-manganese, hemin, diethyldithiocarbamic acid complexes or an iron hemoprotein, in the manufacture of a medicament for the therapy of septic shock The use of transition metal complexes in the treatment of septic shock, in particular the hypotension associated therewith and pharmaceutical formulations comprising such complexes are disclosed. The use of such transition metal complexes in the treatment of other conditions caused by pathological NO production are also disclosed.
WO2005097121A1 Angiogenesis-affecting compounds and methods of use thereof Angiogenesis may be affected by administering a compound to a group of cells, a tissue or an organism. Such affect may be to inhibit or stimulate angiogenesis. The compounds may be used to treat disease states related to insufficient or unregulated angiogenesis.
WO2013048610A1 Contraceptive compositions and methods of contraception Compositions and methods for contraception are disclosed that use 1 - bromopropane.
CN1861090A Toxicity-expelling fibrous nutrient and its prepn. method A detoxicating fibrous nutrient for losing weight without damage to health is proportionally prepared from glucomannan, VA, VB1, VB2, VB6, VC and VE through proportional mixing, spraying the aqueous solution of xylitol and sweet orange essence, stirring, granulating and drying.
CN102690238A Synthesis of barbituric acid derivative as RSK2 inhibitor and application thereof The invention relates to a compound as shown in the general formula I, its pharmaceutically acceptable salt, a prodrug and a solvate, its application in preparation of drugs for treating or preventing RSK2-mediated diseases and its application in preparation of drugs for inhibiting RSK2 activity.
CA2732266A1 Treating various disorders using trkb agonists Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or heterocycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject is provided, which includes selecting a subject in need of neuroprotection, and administering to the subject a therapeutically effective amount of the described compounds.
US20090012150 Stablized Pharmaceutical Composition Comprising an Amorphous Active Substance The invention relates to the pharmaceutical composition comprising the amorphous active substance which is atorvastatin calcium. The process of stabilization of the pharmaceutical composition comprising the pharmaceutical formulation with amorphous atorvastatin calcium, the process of stabilization of the pharmaceutical formulation comprising amorphous atorvastatin calcium and the process of stabilization of atorvastatin calcium in an amorphous form is described.
US20140099378 Modified Release Formulations of Anti-Irritability Drugs Modified or extended release formulations containing mesalamine compounds and associated methods are disclosed and described. In some aspects, such formulations may be substantially bioequivalent to known FDA approved mesalamine formulations such as PENTASA®.
CN101862311A Penetration promoting and eyesight improving eye drop The invention relates to an eye drop, in particular to a penetration promoting and eyesight improving eye drop. The invention aims to solve the problem of treatment period prolongation of an eye disease due to less effective components of the traditional eye drop, which really enter the inner side of an eyeball, by the isolation of a blood-eye barrier, a cornea barrier and an eye surface barrier. A penetration promoting and eyesight improving medicament in the first scheme is any combination of one or more of borneol, menthol, taurochenodeoxycholic acid or tauroursodeoxycholic acid; and a penetration promoting and eyesight improving medicament in the second technical scheme is any combination of one or more of borneol, menthol, chenodeoxycholic acid or ursodesoxycholic acid. The eye drop is used for a patient with conjunctivitis, keratitis and uveitis and used as a penetration promoting agent of other eye drops or an ophthalmic pharmaceutical partner for increasing the amount of the eye drops dropping in eyes. The eye drop can penetrate through the blood-eye barrier, the cornea barrier and the eye surface barrier; and compared with the prior art, the invention can improve the effective component entering the inner side of the eyeballs by 10-200 percent.
WO2013070998A1 TREATMENT OF OVARIAN CANCER WITH 2-AMINO-4H-NAPHTHO[1,2-b]PYRAN-3-CARBONITRILES Methods for inhibiting the growth of ovarian cancer cells or other serosal cancer cells are disclosed. The method involves exposing the cells to a 2-amino-4H-naphtho[1,2-b]pyran-3-carbonitrile of formula. (I). wherein Y is CR1 or N and Z is CR5 or N.
US20120220640 Methods of treating diseases The present invention relates to computer-implemented methods and system for analysing a biomarker which cycles in a subject. In some other aspects, the present invention relates to analysing a biomarker which at least initially increases or decreases in amount in a subject following a treatment for a disease. In further aspects, the present invention relates to computer-implemented methods and systems for determining a preferred time to administer a therapy to treat a disease in a subject. The present invention also relates to computer program product to implement the methods. Further, the present invention relates to methods of determining the timing of treating a disease in a subject in which the immune system is cycling.
US8614213 Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.
US20110250186 Methods for promoting wound healing and muscle regeneration with the cell signaling protein nell1 The present invention provides methods for promoting wound healing and treating muscle atrophy in a mammal in need. The method comprises administering to the mammal a Nell1 protein or a Nell1 nucleic acid molecule.
US7115780 For therapy of ulcers, pancreatitis, obesity, urinary incontinence and pollakiuria The invention concerns compounds of formula (I), wherein A is a group of formula (a) or (b), wherein: R represents a hydrogen or halogen atom, a —S(O)z(C1–C4)Alk wherein z is 0, 1 or 2, a —NHSO2(C1–C4)Alk, —SO2NH(C1–C4)Alk, —NHSO2—(C1–C4)Alk-phenyl or —NHSO2-phenyl group, said phenyl capable of bearing a halogen atom, a (C1–C4)Alk group or a (C1–C6)alkoxy group; R1 represents a hydrogen atom or a —(C1–C4)Alk, —CO(C1–C4)Alk, —(C1–C4)Alk-phenyl or —CO-phenyl group, said phenyl capable of bearing a halogen atom or a —(C1–C4)Alk or (C1–C6)alkoxy group; R2 is a hydrogen atom, a —SO2(C1–C4)Alk, —SO2—(C1–C4)Alk-phenyl, —SO2-phenyl group, or a —(C1–C4)Alk group; X completes a saturated or unsaturated cycle of 5 to 8 atoms, capable of bearing one or two —(C1–C4)Alk groups and/or two carbonyl groups; R3 and R′3 represent each independently a hydrogen or halogen atom, a —(C1–C6)Alk, hydroxy, —CN, —(C1–C6)alkoxy, —COR4 or Y—CR8R9—COR4 group; Y represents O or CH2; R4 represents a hydroxy, (C1–C6)alkoxy or —NR5R6 group; R5 and R6 independently represent a hydrogen atom, a —(C1–C4)Alk, group, aryl or heteroaryl optionally substituted by a R7 group, aralkyl or heteroaralkyl optionally substituted by a R7 group; or R5 and R6, with the nitrogen atom which bears them, form a saturated or unsaturated cycle of 5 to 7 atoms optionally substituted by a R7 group; and R7 represents a hydrogen or halogen atom, a hydroxy, —(C1–C4)Alk, —(C1–C6)alkoxy, —NH(C1–C4)Alk, —N(C1–C4)Alk2, —COO(C1–C4)Alk, aralkyl or heteroaryl group; R8 and R9 independently represent a hydrogen atom or a —(C1–C4)Alk group; their salts or solvates, the pharmaceutical compositions containing them, a method for preparing them and synthesis intermediates
US20080182838 (5-{5-[4-(2-Bromo-5-fluorophenoxy)piperidin-1-yl]pyrazin-2-yl}-2H-tetrazol-2-yl)acetic acid; metabolic disorders,antidiabetic, hypoglycemic agent; obesity, insulin resistance, liver steatosis, atherosclerosis, neurological disease, dyslipidemia, hyperlipidemia, low HDL, and high LDL Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
US8709409 Method for treating rheumatoid arthritis by administering an anti-IL-6 antibody and methotrexate A pharmaceutical composition for the treatment of interleukin-6 (IL-6) related diseases, comprising an interleukin-6 antagonist (IL-6 antagonist) and immunosuppressants. The IL-6 antagonist is preferably an antibody to an interleukin-6 receptor (IL-6R).
US20080113934 Administering formulation containing pyrimido-pyrimidine selected from dipyridamole, mopidamol in combination with an agent selected fromacetylsalicylic acid (ASA), clopidogrel, ticlopidine; strongly influencing the interaction of the vessel wall with the fibrin pathway of the coagulation system A method of treatment of the human or non-human animal body for treating fibrin-dependent microcirculation disorders is disclosed, for example, microcirculation disorders caused by metabolic diseases, inflammatory reactions or autoimmune diseases; peripheral microcirculation disorders or microcirculation disorders associated with increased cell fragmentation comprising administering to a human or non-human animal body in need of such treatment an effective amount of a pharmaceutical composition containing a pyrimido-pyrimidine selected from dipyridamole, mopidamol and the pharmaceutically acceptable salts thereof, and the use of said pyrimido-pyrimidine for the manufacture of a corresponding pharmaceutical composition.
US20090156540 Method for diagnosing and/or predicting the development of an allergic disorder and agents for treating and/or preventing same The present invention relates to genes whose level of expression is different in allergic animals compared with non-allergic animals. In particular, the present invention relates to a method for predicting the development of an allergic disorder in a mammal by determining the gene expression pattern of a panel of specific sequences comprising CAMK2D and CDH1 within a nucleic acid pool that have been predetermined to either increase or decrease in response to allergy.
WO2014139033A1 Compounds and compositions for drug release The invention relates to compounds that include biologically active agents (e.g., compounds according to any of formulas (I) and (I-A) that can be used for effective drug release, e.g., as coatings for medical devices. Use of these compounds in the coating of surfaces can allow for long-term drug release as well as imparting uniform coatings with little phase separation compared to, e.g., the parent biologically active agent.
US20120214848 [1,2,4]oxadiazol-3-yl acid salts and crystalline forms and their preparation The present invention relates to salts and crystalline forms of [1,2,4]oxadiazol-3-yl]-phenoxy}-cycloalkyl carboxylic acids, processes for their preparation, pharmaceutical compositions comprising such compounds, and methods of using them.
EP2785689A1 Amorphous ezatiostat ansolvate Provided herein is an amorphous form of a pharmaceutically acceptable salt of ezatiostat, for example, ezatiostat hydrochloride, compositions, uses and methods of preparation thereof.
CN102526076A Animal application of aspirin derivative The invention relates to an animal application of an aspirin derivative, in particular to application of the aspirin derivative in inhibiting prostaglandin generation of animals. The aspirin derivative is a preparation prepared from aspirin arginine, lysine, calcium salt, sodium salt or magnesium salt and includes an oral powder preparation, an injection, injection powder, oral tablets and the like. The preparation can be used for pets including dogs, cats and the like and food animals including pigs, cattle, birds and the like and used for reducing fevers, easing pains, resisting inflammation and relieving urate depositions.
CN103333218A 3 alpha,11 alpha-dihydroxy-lupin-20(29)-alkene-28-acid with anti-inflammatory effect and preparation method thereof The invention discloses a lupane-type triterpene 3 alpha,11 alpha-dihydroxy-lupin-20(29)-alkene-28-acid (impressic acid) with an anti-inflammatory effect, and a preparation method thereof. The impressic acid has an advantage of good anti-inflammatory effect. The preparation method has advantages of mild conditions, simple operation steps, high extraction effect and high product purity.
CN102028665A Nimodipine oral fast dissolving tablets and preparation method thereof The invention belongs to the field of medicinal preparations. Nimodipine serving as a clinical cerebrovascular medicament is applied for years; however, the nimodipine has the defects of poor water solubility, obvious first pass effect and the like due to the physicochemical property of the nimodipine, which directly influence clinical medicinal effect. The invention provides nimodipine oral fast dissolving tablets and a preparation method thereof. The preparation method comprises the following steps of: preparing a nimodipine solid dispersion with high water solubility from a nimodipine raw material and a hydrophilic carrier by a spray drying process; mixing the solid dispersion and suitable auxiliary materials; and preparing the oral fast dissolving tablets by a direct powder compression method. The preparation process is simple and industrial production is easy to realize. The prepared nimodipine oral fast dissolving tablets can be administrated without water. After being administrated, the nimodipine oral fast dissolving tablets are rapidly dissolved and absorbed in an oral cavity in 30 seconds so as to avoid the first pass effect of the gastrointestinal tract, greatly improve the dissolution rate of the medicament and improve the bioavailability of the medicament.
CN102406544A Azithromycin lactobionateinjection solution packaged by double-cavity bag and preparation method The invention discloses an azithromycin lactobionateinjection injection solution packaged by double-cavity bag. The medicinal composition of the injection solution comprises the following raw materials: 0.1-0.3 parts by weight of azithromycin lactobionateinjection in a powder cavity, and 4-11 parts by weight of glucose injection solution with 100 parts by volume of glucose or 0.8-1 parts by weight of sodium chloride injection solution with 100 parts by volume of sodium chloride in a solution cavity. The azithromycin lactobionateinjection injection solution is packaged by a double-cavity bag; sterilized azithromycin lactobionateinjection powder and solvent (sodium chloride injection solution or glucose injection solution) are filled in two cavities separated by pseudo soldering separations respectively; and when the azithromycin lactobionateinjection injection solution is used, pseudo soldering isolating bars can be connected by extruding a medicine bag only, and the sterilized azithromycin lactobionateinjection powder and the solvent are quickly solved and mixed under the sealed and sterilized condition to form a total medicine treatment mixed solution which can be directly applied to the patient.
WO2008123231A1 Novel cyclic staple-type oligonucleotide, and nf-κb decoy comprising the same Disclosed is a novel oligonucleotide which is highly capable of binding to NF-κB compared to a conventional oligonucleotide decoy for NF-κB, and is therefore useful as a NF-κB decoy. Also disclosed is use of the oligonucleotide for medical purposes. The oligonucleotide is a cyclic staple-type oligodeoxynucleotide composed of a stem structure and two loop structures attached to both termini of the stem structure, wherein the stem structure comprises a double-strand composed of two chains, and each of the two chains comprises a consensus sequence and a 5'-addition sequence and a 3'-addition sequence each having a specific nucleotide sequence and attached to both termini of the consensus sequence. The cyclic staple-type oligodeoxynucleotide is useful as a prophylactic, ameliorating or therapeutic agent for an ischemic disease, an allergic disease, an inflammatory disease, an autoimmune disease, metastasis/invasion of cancer, or cachexia.
CN103655517A Pep-1 peptide modified gliomas targeted nano drug delivery system and preparation method thereof The invention discloses a Pep-1 peptide modified gliomas targeted nano drug delivery system and a preparation method thereof. The nano drug delivery system comprises polymer nano particles prepared by using an amphiphilic block copolymer (Pep-PEG-PLGA) as a carrier material, paclitaxel wrapped and carried by the polymer nano particles, and modified ligand Pep-1 polypeptide on the surfaces of the polymer nano particles. The amphiphilic block copolymer (Pep-PEG-PLGA) is composed of Male-PEG-PLGA and MePEG-PLGA, Pep-1 is adopted as a molecule with targeting function, the amphiphilic block copolymer PEG-PLGA is taken as a carrier material, the Pep-1 polypeptide is modified on the carrier material via covalent binding, and gliomas targeted polymer nano particles are prepared. According to the Pep-1 peptide modified gliomas targeted nano drug delivery system, gliomas targeting can be voluntarily performed, and the uptaking and accumulation of an anti-tumour drug in the gliomas part can be improved, as a result, the gliomas therapeutic effect is improved.
CN1813836A Medicinal composition for treating cardio-cerebrovascular disease The present invention discloses a medicine composition for curing angiocardiopathy and cerebrovascular disease and its preparation. It is formed from ligustrazine, notoginseng total saponin and borneol according to the mixing ratio of 1:0.1-10:0.1-0.01. Said medicine composition can be made into oral preparation and injection preparation.
US8748406 Preventive for adhesion following abdominal surgery The present inventors discovered that oligonucleotides which suppress midkine expression and antibodies which suppress midkine activity can be used to prevent post-surgical intraperitoneal adhesions.
CN103169850A Mongolian medicine for treating peptic ulcer The invention relates to a drug, namely a mongolian medicine for treating peptic ulcer. The mongolian medicine is characterized in that the drug is prepared from the following crude drugs in parts by weight: 2-6 parts of kanako, 3-9 parts of angelica sinensis, 2-6 parts of trogopterus dung, 5-12 parts of gypsum rubrum, 5-12 parts of myrobalan, 5-12 parts of cuttlebone, 2-6 parts of bulb of fritillary, 2-6 parts of coptis chinensis and 1-5 parts of elecampane. The anaesthetic has the beneficial effects of being significant in curative effect on the peptic ulcer, short in course of treatment, fast to become effective, free of poison and side effects, easy to obtain materials, simple to prepare, low in cost, convenient to use, and wide in application range. Therefore, the mongolian medicine has high use value and a wide market prospect.
CN101919906A Novel application of salvianolic acid compound as water-soluble component in salvia miltiorrhiza extract The invention relates to novel application of a salvianolic acid compound as a water-soluble component in a salvia miltiorrhiza extract, wherein the salvianolic acid compound is selected from a salvianic acid A sodium compound in a formula 1, a rosmarinic acid compound in a formula 2 and a salvianolic acid B compound in a formula 3 or a composition thereof. The salvianolic acid compound has the function of blocking the combination of CD36 and the relevant ligands thereof as a CD36 antagonist, wherein the relevant ligands of the CD36 include, but not limited to oxidized low-density lipoprotein (oxLDL), acetylized low-density lipoprotein (acLDL), advanced glycation end products (AGE), thrombospondin 1 (TSP-1), growth hormone releasing peptide (GHRP), long-chain fatty acid (LCFA), beta-Amyloid (Abeta), low-density lipoprotein (LDL), high-density lipoprotein (HDL), very low-density lipoprotein (VLDL), plasmodium-infected red blood cells, apoptotic neutrophils, and the like. The invention also relates to application of the salvianolic acid compound in the preparation of medicaments for blocking the combination of the CD36 and the relevant ligands thereof.
CN101434557A Derivative of short chain 2-hydroxy carboxylic acid of ceramide The invention relates to a compound, which is analog sphingosine base selected from sphingosine which is connected to 2-hydroxy-carboxyl with a chain length of 2 to 14 carbon atoms by amides and sphingosine, and the condition is that the compound is not glycolyl Sphingosine, 2-hydroxy butyryl group sphingosine or 2-hydroxy decanoyl dihydro sphingosine. The invention also relates to a preparation method of the compound, cosmetics or medical composition containing the compound, therapeutic application of the compound and the application of the compound as cosmetics.
CN102764234A Topotecan hydrochloride targeted liposome preparation and preparation method thereof The invention provides a topotecan hydrochloride targeted liposome preparation and a preparation method of the topotecan hydrochloride targeted liposome preparation. According to the topotecan hydrochloride targeted liposome preparation, antitumor drug topotecan hydrochloride is encapsulated into a targeted long-circulating liposome modified by hydrophilic polymer polyethylene glycol and targeted ligand RGD cyclopeptide, and the lipsome is capable of prolonging the circulating time of the medicine in the body, thereby the tumor targeting is achieved, the curative effect is improved and the toxic and side effects are reduced.
WO2006052013A1 Thienopyrrole compounds and utilization thereof as hcv polymerase inhibitor A thienopyrrole compound represented by the general formula [I]: [I] wherein each symbol has the meaning as defined in the description; or a pharmaceutically acceptable salt thereof; and a hepatitis C virus (HCV) polymerase inhibitor and a remedy for hepatitis C containing the compound as the active ingredient. Because of exerting an anti-HCV effect based on an effect of inhibiting HCV polymerase, the above compound is useful as a remedy or a preventive for hepatitis C.
CN102648905A Combined medicament for treating swine pneumonia and upper respiratory tract infection and preparation method thereof The invention relates to a combined medicament for treating swine pneumonia and upper respiratory tract infection and a preparation method thereof. The composition mainly comprises kalii dehydrographolidi succinas, tylosin, sodium hydrogen phosphate, beta-mercaptoethanol, propylene glycol and water for injecting. The combined medicament has the advantages of high stability, simple and convenient process, synergic action among major components, enhanced medicinal effect and good treatment effects on swine bacterial and viral pneumonia and upper respiratory tract infection.
US7763729 Bicyclic heteroaromatic derivatives Bicyclic heteroaromatic derivatives of formula (1) are described: F(1) where: the dashed line joining A and C(Ra) is present and represents a bond and A is a —N═ atom or a —C(Rb)═ group, or the dashed line is absent and A is a —N(Rb)—, or —C(Rb)(Rc)— group; X is an —O—, —S— or substituted nitrogen atom or a —S(O)—, —S(O2)— or —NH-group; Y is a nitrogen or substituted carbon atom or a —CH═ group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the remaining substituents are defined in the specification. The compounds are potent and selective inhibitors of p38 kinase and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
US7618652 Glycosaminoglycan anticoagulants derived from fish The present invention provides anticoagulant piscine gill glucosaminoglycans, high affinity anticoagulant piscine glycosaminoglycans anticoagulant glycosaminoglycans extractable from salmon guts, skin, tail or gills and salts and derivatives thereof.
EP1852503A1 Il-13 production inhibitor The present invention provides a screening method/screening kit for an IL-13 production inhibitor, which comprises using (a) a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or its partial peptide, or a salt thereof; and (b) a ligand capable of specifically binding to the protein; an IL-13 production inhibitor which is obtainable by said screening, and the like. The IL-13 production inhibitor which can be obtained by the screening of the present invention is useful as a prophylactic/therapeutic agent for, e.g., respiratory disease, etc.
US20100137449 Substituted 1,3-cyclopentadione multi-target protein kinase modulators of cancer, angiogenesis and the inflammatory pathways associated therewith Compounds and methods for multi-targeted protein kinase modulation for angiogenesis, cancer treatment or the inflammatory pathways associated with those conditions are disclosed. The compounds and methods disclosed are based on substituted 1,3-cyclopentadione compounds.
CN103339141A C-28 amines of c-3 modified betulinic acid derivatives as hiv maturation inhibitors Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS. In particular, the following compounds are provided herein, including pharmaceutically acceptable salts thereof: a compound of formula (I), a compound of formula (II), and a compound of formula (III).
CN101836977B Extract of Morus australis Poir. and antibacterial application of Kuwanon H compound The invention relates to an extract made of Morus australis Poir. root bark and antibacterial application of Kuwanon H compound which is separated from the extract and has a structure as shown in a formula (I).
US20130225546 Novel synthetic procedure and cancer treatment with cisplatin derivatives A method of reducing the in vivo viability of cancer cells selected from the group consisting of breast cancer cells, lung cancer cells, prostate cancer cells and melanoma cancer cells has steps of: a) identifying a prospective patient having cancer cells selected from the group consisting of breast cancer cells, lung cancer cells, prostate cancer cells and melanoma cancer cells; and b) administering a cisplatin derivative to the prospective patient so that the cisplatin derivative will contact the cancer cells; wherein the cisplatin derivative is a 4,4′-bis[RO]-2,2′-bipyridine)PtCl2 where, R is selected from the group consisting of —(CH2)nCH3 where n=2, 3, 4 or 5, and —(CH2)n[O(CH2)m]yO(CH2)zCH3 where n=2, m=2, y=2, z=1. A novel synthetic process for the manufacture of these compounds (and their analogs) is also provided.
CN103601732A Nitrogen-substituted podophyllotoxin derivative with anti-tumor activity and preparation method and use thereof The invention discloses a nitrogen-substituted podophyllotoxin derivative with anti-tumor activity and a preparation method and use thereof. According to the method, 2-aminopyrimidine, 2-aminopyridine, 2-amino-3-methylpyridine, 2-amino-4-methylpyridine, 2-amino-5-methylpyridine, 2-amino-4,6-dimethyl pyridine, 3-aminopyridine, 3-amino-4-methylpyridine, 5-amino-2-methylpyridine, 3-amino-2-chloropyridine or 4-amino-2-chloropyridine is respectively introduced to an activated C-ring fourth position of a podophyllotoxin compound through nitrogen substitution reaction, so as to obtain the nitrogen-substituted podophyllotoxin derivative, represented by a formula (V) shown in the specification, with excellent anti-tumor activity. The nitrogen-substituted podophyllotoxin derivative disclosed by the invention acts on tumor cells through multiple ways and multiple target points, and the anti-tumor activity of the nitrogen-substituted podophyllotoxin derivative is remarkably improved compared with that of the podophyllotoxin compound. The compound disclosed by the invention can be used for preparing anti-tumor drugs and is clinically applied to anti-tumor treatment.
WO2011072398A1 Local delivery of drugs from self assembled coatings The invention relates to oligofluorinated coatings and their use in drag delivery The oligofluorinated coatings are compositions comprising formula (XVII). These coatings are used in a method of delivering a biologically active agent to a tissue surface in a mammalian tissue This method occurs by contacting the surface with the coating including an oligofluorinated oligomer and a biologically active agent wherein the coating resides on the tissue surface and release the biologically active agent to the tissue surface.
WO2008137436A1 [6,5]-bicyclic gpr119 g protein-coupled receptor agonists Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n2, n3, n4, A, B, D, E, G, J, Y, R1 and R2 are defined herein.
CN102335132A Asarin inhalation aerosol and preparation method thereof The invention discloses an asarin inhalation aerosol and a preparation method thereof. The asarin inhalation aerosol is prepared from the following raw materials in certain proportions by weight: asarin, propellant, latent solvent, antioxidant, flavoring agent and bacteriostat, wherein the propellant is HFA-134a or HFA-227. The asarin inhalation aerosol effectively solves the problems of low bioavailability and big toxic side effects of oral preparations and injections of asarin. The asarin inhalation aerosol has a simple preparation process, can improve the bioavailability of asarin through oral inhalation, has the advantages of quick effect taking speed, convenience in use, convenience in carrying due to small volume and the like, and can be widely used clinically for treating asthma and chronic obstructive pulmonary disease (COPD), diminishing inflammation, relieving cough, eliminating phlegm, relieving asthma, calming, relieving spasm and treating grand mal and petit mal epilepsy.
CN102973554A Medical application of alantolactone The invention relates to the field of medicine, and in particular relates to medical application of alantolactone. The alantolactone can be used for preventing and treating enteritis.
CN102973525A Antharcycline antitumor antibiotics loaded nano-micelle preparation and preparation method thereof The invention discloses an antharcycline antitumor antibiotics loaded nano-micelle preparation, which comprises antharcycline antitumor antibiotics, A-B-C type triblock polymer and assisting agents, wherein the antharcycline antitumor antibiotics is one or more of adriamycin, daunorubicin, pharmorubicin, perarubicin or lacinomycin; and the A-B-C type triblock polymer is polyethylene glycol-polyethylene glycol containing carboxyl on side chain-polyester. According to the preparation, drugs are coated in the nano-micelle by virtue of the coaction of self-assembly of segmented copolymer and electrostatic adsorption, the nano-micelle has uniform and stable grain diameter, the encapsulation efficiency reaches 99 percent, and the prepared nano-micelle preparation is of a spherical structure with grain diameter between 20 and 300nm; and the shell of the micelle is made from polyethylene glycol molecules, so that drugs are prevented from being contacted with enzyme and other protein molecules in blood or identified and swallowed by a reticuloendothelial system in the body, so that the circulating period of micelle in the body can be prolonged.
CA2624007A1 Acyl indoles, compositions containing such compounds and methods of use The present invention relates to substituted indoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus and related conditions.
US20100184838 Compositions and methods for retinal transduction and photoreceptor specific transgene expression Adenovirus (Ad) vectors are here provided for treatment of ocular tissues as are suitable methods to transduce photoreceptor (PR) cells, the tissue associated with degeneration. Expression from CMV or chicken beta actin (CBA) promoters in neural retina were compared, and CBA was found to be 173-fold more potent than CMV. Further, the RGD domain in Ad penton was found to play a key role in RPE tropism. Deletion of the RGD domain coupled with the CBA promoter permitted transgene expression in neural retina approximately 667-fold more efficiently than with prior Ad5 vectors. Use of Ad vectors in combination with a 4.7 kb rhodopsin promoter enabled transgene expression exclusively in photoreceptor cells in vivo.
CN101574320A Intestinal protection medicament and preparation method thereof The invention provides a bismuth subsalicylate dispersing tablet and a preparation method thereof. The bismuth subsalicylate dispersing tablet is convenient and flexible to take, has an excellent taste, not only can be drunk after being dissolved in water, but also can be directly swallowed or chewed and sucked. The bismuth subsalicylate dispersing tablet as a gastrointestinal medicament can be rapidly disintegrated, has a favorable taste without a sandy feedling and costs little effect for old people, children or patients troublesome in swallowing the medicament. The invention has simple manufacture technology and unique prescription, can fully exert the efficacy of the medicament, is convenient to take and has favorable popularization prospects.
CA2206566C Method and composition for reducing tumor development with a combination of platinum and tellurium or selenium compounds There are provided compositions for, and a method of, treating malignancies which comprise effective amounts of a novel combined therapy comprising a platinum compound and a tellurium or selenium compound, e.g., ammonium trichloro(dioxoethylene-O,O-tellurate), and administering the respective compounds simultaneously or separately.
US20050147670 Oral disintegrating dosage forms The invention is directed to pharmaceutical dosage forms having immediate release via rapid oral disintegration, specifically, orally disintegrating tablets containing levodopa and carbidopa. The invention further provides formulations containing relatively increased amounts of carbidopa than previously available, including, for example, formulations containing carbidopa-levodopa ratios of about 1:1 to about 1:3.
CN101385725A Use of green tea polyphenol in preparing medicine or food for preventing and treating senile memory impairment The invention relates to the use of green tea polyphenols in the preparation of drugs or foods for controlling senile memory decline. The experiments confirm that the green tea polyphenols can prolong the escape latency of C57BL/6J senile mice and SAMP8 mice in a Morris water maze place navigation test, prolong the target quadrant duration in a space exploration test, increase the number of penetration, prolong the latency in a step-down test, reduce the number of errors and increase the active avoidance response rate in a shuttle box test; the results show that the green tea polyphenols can improve the space memory exploration ability, the passive avoidance ability and the active avoidance ability of the mice and have the function of preventing and treating the senile memory decline.
CN103690520A Patch containing essential oil of single leaf asarum, as well as preparation method and medical application of patch The invention relates to a preparation method and medical application of a patch containing essential oil of single leaf asarum, in particular to the essential oil of single leaf asarum belonging to asarum. The preparation method is as follows: a supercritical fluid extracting method is used for extracting the essential oil from single leaf asarum roots and root stocks. The single leaf asarum essential oil is applied to preparation of the patch. The patch consists of a backing layer, a medicated layer and a protective film, wherein the medicated layer consists of 20 to 80% of skeleton-shaped excipients, 15 to 35% of single leaf asarum essential oil, 10 to 20% of transdermal accelerators and 5 to 25% of plasticizers, and is 0.2 to 0.4 cm in thickness. The patch has positive effects of being capable of treating headache or migraine caused by various reasons with exact treatment effect; the patch is good in product stability, accurate in dosage of preparation, high in bioavailability, and convenient to carry and use; the patch overcomes the deficiency of large toxic and side effects and the like of western medicine, and truly realizes the purpose of treating an internal illness by external treatment via transdermal absorption.
CN102503901A Zole antifungal compounds, and preparation method and application thereof The invention relates to the technical field of medicines, in particular to zole antifungal compounds, and a preparation method and application thereof. The compounds have a chemical structural general formula shown in the specifications, wherein R is one or more of hydrogen, C1-4 alkyl, halogen, cyan, nitro, amino and C1-4 alkoxy, and n is an integer ranging from 1 to 5. The compounds have high antifungal activity; and compared with the conventional antifungal medicines clinically applied, the compounds have the advantages of high efficiency, low toxicity, wide antifungal spectrum and the like, so the compounds can be used for preparing antifungal medicines.
EP0967985B1 Process for improving glucose metabolism, satiety, and nutrient absorption in companion animals A process for feeding an animal a diet which alters the function and morphology of the gastrointestinal tract (GIT), a large lymphoid organ in the animal and which improves glucose metabolism, satiety, and nutrient absorption. The process involves feeding a companion animal such as, for example, a dog or cat a diet of a pet food composition containing fermentable fibers which have an organic matter disappearance (OMD) of 15 to 60 percent when fermented by fecal bacteria for a 24 hour period, the fibers being present in amounts from about 1 to 11 weight percent of supplemental total dietary fiber. The animal is maintained on the diet for a sufficient period of time to allow the fermentable fibers to ferment in the GIT of the animal.
US20120225924 Single-monomer derived linear-like copolymer comprising polyethylenimine and poly(ethylene glycol) for nucleic acid delivery A method of synthesizing a random copolymer of polyethyleneimine and polyethylene glycol, comprising exposing ethanolamine in a solution to electromagnetic radiation for a sufficient time to polymerize the ethanolamine (OHCH2CH2NH2) and thereby resulting in formation of the randome copolymer comprising polyethyleneimine and poly(ethylene glycol), wherein the polyethyleneimine comprises ethyleneimine (—CH2CH2NH—) unit and the polyethylene glycol comprises ethylene glycol (—CH2CH2O—) unit, and the polyethylenimine of the random copolymer has a substantially linear backbone.
US20130045172 USE OF CIS-EPOXYEICOSATRIENOIC ACIDS AND INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE TO TREAT CONDITIONS MEDIATED BY PBR, CB2, and NK2 RECEPTORS The invention relates to the discovery that cis-epoxyeicosatraenoic acids (EETs) bind to and act as agonists of peripheral benzodiazepine receptor and the cannabinoid CB2 receptor. The invention provides methods of reducing symptoms of conditions whose activity is mediated by these receptors, including inhibiting anxiety, inhibiting the growth of cancer cells expressing peripheral benzodiazepine receptors, and reducing oxygen radical damage to cells, by contacting the cells with a cis-epoxyeicosantrienoic acid, an inhibitor of soluble epoxide hydrolase (sEH), or both. The invention further provides methods of inhibiting irritable bowel syndrome by administering to individuals with inhibiting irritable bowel syndrome a cis-epoxyeicosantrienoic acid, an inhibitor of soluble epoxide hydrolase (sEH), or both. In some embodiments, the method comprises administering to the individual a nucleic acid which inhibits expression of sEH.
US7674887 3'-{N'-[1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1,5-dihydropyrazol-4-ylidene]hydrazino}-2'-hydroxybiphenyl-3-carboxylic acid; thrombocytopenia and megakaryocytopoiesis treatment Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.
US7064137 Analgesics; anxiolytic agents; gastrointestinal disorders Compounds of general formula (I): R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6 alkyl, NO2, CF3, C1–C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.
US7074437 comprises synthetic zeolite, protein extracts of nettle, milk vetch, balm, hop cones, and B-complex vitamins The increased level of glucose in blood is the result of the destruction of β cells of the Islets of Langerhans by autoimmune process in insulin-dependent form of diabetes or a relative lack of insulin in insulin-dependent form of diabetes. Constantly present hyperglycemia in diabetes and a relative lack of insulin aid the development of the neuropathy as a late complication of diabetes. For that purpose, a technical problem was set before the inventor with the request of the reduction of glucose in blood, and stopping of the process of the development of the neuropathy as the consequence of the “long” duration of diabetes. Such a mineral-protein preparation was prepared by which glycemia was successfully regulated, but the process was also stopped by depositing of Ca+ in nerve cells. Those early changes caused by diabetes were successfully stopped, so that the appearance of the neuropathy, as a late complication in diabetes, was postponed. The mineral-protein preparation showed a hypoglycemia effect and stopped the development and progressing of the diabetic neuropathy.
CN103254184A 5-substituted-3-[5-hydroxy-4-pyrone-2-yl-methylmercapto]-4-amino-1,2,4-triazole compound and application thereof The invention provides a novel 5-substituted-3-[5-hydroxy-4-pyrone-2-yl-methylmercapto]-4-amino-1,2,4-triazole compound shown as formula (I), wherein in the formula (I), a substituent R is one of -CH3, -CH2CH3, -CH2CH2CH3, C6H5-, 3-CH3C6H4, 2-CH3C6H4, 4-CH3C6H4, 2-CH3OC6H4, 4-CH3OC6H4, 2-ClC6H4, 4-ClC6H4, 3-ClC6H4, 3-BrC6H4, 4-BrC6H4, 3-FC6H4, 4-FC6H4, 3-NO2C6H4, 4-NO2C6H4, 3-CNC6H4, 4-CNC6H4, 3-F3CC6H4 and 4-F3CC6H4. The 5-substituted-3-[5-hydroxy-4-pyrone-2-yl-methylmercapto]-4-amino-1,2,4-triazole compound has certain inhibitory activity for tyrosinase, a synthesis method is simple, and materials are easy to obtain. The novel 5-substituted-3-[5-hydroxy-4-pyrone-2-yl-methylmercapto]-4-amino-1,2,4-triazole compound can be used for preparing cosmetics or medicaments for whitening or inhibiting melanogenesis.
WO2012136317A1 Rosmarinic acid for smoker dehabituation The present invention relates to rosmarinic acid for use in a method for smoker dehabituation, wherein the rosmarinic acid is preferably present in the form of a dried aqueous extract of lemon balm (Melissa officinalis). In addition, the present invention relates to foods and food supplements for use in a method for smoker dehabituation, wherein these food and food supplements contain rosmarinic acid, in particular rosmarinic acid in the form of a dried aqueous extract of leaves of lemon balm (Melissa officinalis).
CN101077333A External applied gel with butenafine hydrochloride as principal ingredient The present invention provides one kind of externally applied gel preparation with butenafine hydrochloride as the main component and supplementary materials. The externally applied gel preparation is used in treating fungus infection caused tinea manuum, tinea pedis, tinea corporis, tinea cruris and tinea versicolor. It has the advantages of high stability, convenient use, high patient' s compliance, etc. The present invention provides one new preparation form of butenafine hydrochloride for clinical application.
CN103385875A Nanometer chitosan artemisinin compound and preparation method thereof The invention discloses a nanometer chitosan artemisinin compound that comprises, based on weight percentage, the following components: 40%-80% artemisinin or artemisinin derivatives; 1%-5% of polyvinyl pyrrolidone, and 15%-50% of nanometer chitosan. The nanometer chitosan artemisinin compound prepared by the invention is water-soluble artemisinin with good solubility, and can be easily absorbed by human body with no toxic and side effect; the nanostructured of which has slow release effect; the medicament half life is substantially improved; the feeding frequency is reduced; the patient compliance is increased; the drug resistance is prevented from forming; the biology utilization rate of artemisinin and derivatives are raised; and the treatment effect is increased.
WO2008116813A3 Combination medicaments for treating bacterial infections Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C=N-O- has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.
CN101143134A Dexrazoxane freezing-dried powder injection and preparation method thereof The invention relates to a dexrazoxane freeze-dried powder injection and the preparation method. The preparation is used for resisting the cardiac toxicity which is induced by the cumulate quantity of adriamycin. The dexrazoxane freeze-dried powder injection contains the active components of the dexrazoxane and hydrochloric acid, the weight proportion of which is 1 to 0.05 to 0.5, and the preferential proportion is 1 to 0.2 to 0.5. The preparation method is that the hydrochloric acid is put into an aseptic vessel; the water for injecting is added till 80 percent of the preparation quantity, and the temperature is reduced and kept at 2 to 6 DEG C; the dexrazoxane is added to be mixed, and the hydrochloric acid of 1.0mol/L is dripped slowly into the solution to be solved while mixing the solution; the water for injecting is added till the full quantity; active carbon of 0.3 percent is added for absorbing for thirty minutes, and then the solution is decarbonized; after the medium body content is mensurated as being eligible, the solution is filtered by a 0.22 micron-micropore filtering filer; the filtrate is filled into a 25ml cillin bottle according to the filling quantity of 10ml each bottle, and the bottles are partially plugged by buna plugs and filled onto a plate to be sent into a freeze-drying box; a temperature probe is inserted, and the box door is closed; the filtrate is warmed, sublimed and dried be stages; nitrogen is puffed; the plugs are pressed; the filtrate is taken out from the box for rolling the openings, detecting the quality and packaging and the preparation can be obtained.
EP1973872A1 Inhibitors of histone deacetylase and prodrugs thereof The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
US20090082437 Use of Oxaliplatin for Enhancing Radiosensitivity in Radiotherapy of Cervical Cancer The present invention relates to a method for enhancing radiosensitivity in radiotherapy of cervical cancer by administering to cervical cancer cells an effective amount of oxaliplatin. Radiation combined with pretreatment of oxaliplatin according to the present invention helps to enhance the cytotoxicity of radiation and result in augmenting radiation-induced mitotic catastrophe. The analysis on molecular mechanism revealed that oxaliplatin augmented the radiation-induced DNA double-strand break indicated by reducing gamma-H2AX expression, abrogated radiation-induced ATM phosphorylation and reduced the Chk2 phosphorylation. Oxaliplatin can be used as a promising radiosensitizer for treatment of cervical cancer in radiotherapy.
EP1499598A1 Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions The present invention concerns chemical compounds combining affinity and antagonism against the human m3 muscarinic receptor with activity as selective phosphodiesterase IV (PDE IV) inhibitors, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
CN103554134A Chromone structure containing isoxazole norcantharidin derivatives as well as preparation method and application thereof The invention discloses novel chromone structure containing isoxazole norcantharidin derivatives as well as a preparation method and an application thereof. The preparation method is characterized by introducing isoxazole rings to C5 and C6 in a norcantharidin structure by using a 1,3-dipolar cycloaddition method to react with chromone derivatives to import the chromone structures, thus synthesizing a series of totally six novel chromone structure containing isoxazole norcantharidin derivatives. The isoxazole norcantharidin derivatives are applied to synthesis of antitumor drugs and have broad application prospects.
WO2009155118A1 Compositions and methods for inactivation of pathogens at genital tract surfaces The present disclosure includes compositions and methods of inactivating pathogens of a genital tract of a female. The compositions include L-lactic acid substantially free of D-lactic acid.
US20080255225 Botanical Extract Composition The invention relates to a kit comprising: a first composition comprising leaves of Melissa Officinalis, or parts thereof; a second composition comprising Eleutherococcus senticosus, or parts thereof; a third composition comprising Avena sativa, or parts thereof; a fourth composition comprising Ballota Nigra, or parts thereof; a third composition comprising the roots of Glycyrrhiza glabra/gan cao, or parts thereof; and a sixth composition comprising roots of Uncaria Tomentosa, or parts thereof. The invention further relates to a kit for use as a medicament, to a kit for use in the treatment of disorders in mammals, like humans, horses, cows, pigs and pets, to a kit for use in the treatment of lupus, multiple sclerosis, rheumatoid arthritis, rheumatism, osteoporosis, asthma in humans or tale and mane eczema in horses, and to the use of the kit for the treatment of lupus, multiple sclerosis, rheumatoid arthritis, rheumatism, osteoporosis, asthma in humans or tale and mane eczema in horses.
WO2007049575A1 Taxane compound with azetidine ring structure A compound represented by the general formula (1) having a high antitumor effect on a cancer cell including a drug-resistant cell. [X1 and X2 represents a hydrogen atom, a halogen atom, a hydroxyl group or the like, R1 represents a phenyl group, R2 represents an alkyl group, an alkenyl group or an alkoxy group, R3 represents a hydrogen atom, a halogen atom, a hydroxyl group or an alkoxy group, R4 represents a hydrogen atom or an alkyl group, Z1 and Z2 represent a hydrogen atom, a halogen atom a hydroxyl group or the like, Z3 represents a cyano group, an alkyl group, alkenyl group or the like, Z4 represents an alkyl group, an alkenyl group, an alkynyl group or the like, and --- represents a single bond or a double bond.]
CN101602657A Halogenated hydroxyl arone compounds, preparation method and use thereof The invention relates to novel compounds, a preparation method and use thereof, in particular to halogenated hydroxyl arone compounds, a preparation method and use thereof, which solves the problem that halogenated hydroxyl arone lead compounds from natural sources are high in extraction cost, low in yield and difficult to develop follow-up study. The compounds have a structural formula on the right, wherein R1' is one or more hydroxyl or hydrogen atoms in any position on an A ring; R2' is one or more hydroxyl or hydrogen atoms in any position on a B ring; and X is one or more halogen or hydrogen atoms in any position on the A ring or the B ring. A synthesis method has the advantages of mild reaction conditions, widely readily available raw materials, simple preparation method, high yield, low cost and the like, and is suitable for industrial production. The synthesized halogenated hydroxyl arone compounds and non-toxic salts, ester and ether thereof have the activity of resisting bacteria, tumors, oxidation and vascular endothelial cell injury and inhibiting proliferation of vascular smooth muscle cells.
US20130065843 Phenolic Compositions Derived From Apple Skin And Uses Thereof Described herein are phenolic compositions derived from apple skins. In particular, described herein are flavonoid-rich fractions derived from apple skin extract. The compositions are useful in the prevention and treatment of conditions associated with oxidative stress and/or inflammation, including certain neurodegenerative diseases. Methods of producing the compositions are also described.
US20090123567 1,2-Bis[(1,2)-benzisoselenazol-3(2H)-onyl]ethane; high anti-oxidative activity and low toxicity; in combination with other anticarcinogenic, anticoagulant, antiinflammatory agents ( cisplatin, adriamycin, taxol; aspirin; indometacin) The present invention relates to new bisbenzisoselenazolonyl derivatives of the following general formula (I), wherein R is C4-5-alkylene, and their pharmaceutically acceptable salts. The inventive derivatives have antineoplastic, anti-inflammatory and antithrombotic activities.
US7052684 Methods of healing wounds and fibrotic disorders using IL-10 The present invention provides IL-10 or a fragment or a partially modified form thereof for use in promoting the healing of wounds and fibrotic disorders with reduced scarring and methods for same.
US20050038015 Partial dopamine-D 2 receptor agonist plus serotonin and/oder noradrenaline inhibitor activity The invention relates to the use of a compound or a combination of compounds having partial dopamine-D2 receptor agonistic activity and serotonin and/or noradrenaline reuptake inhibitory activity, for the preparation of a pharmaceutical composition for the treatment of psychiatric and/or neurologic disorders caused by disturbances of the major monoaminergic (dopamine, serotonin and/or nordrenaline) systems or that can be treated via manipulation of those systems.
US20110085975 Hypoxia-selective, weakly basic 2-nitroimidazole delivery agents and methods of use thereof The invention features a class of 2-nitroimidazole compounds with a secondary basic nitrogen atom and a linker bearing one or more therapeutic agents, cytotoxic agents, detectable labels, or chelating groups. In particular, the invention provides 2-nitroimidazole compounds containing a cluster of boron atoms for use in boron neutron capture therapy (BNCT). The 2-nitroimidazole compounds can be used to treat hypoxic conditions, including, e.g., cancer, inflammation, and ischemia. The weakly basic 2-nitroimidazole compounds target to hypoxic tissue and provide increased tissue concentration overall.
WO2013033461A1 Heterocyclic boronic acid ester derivatives and therapeutic uses thereof Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to cyclic boronate compounds and their use as therapeutic agents.
US20110076319 Bioresorbable metal stent with controlled resorption Embodiments herein relate to a special form of a bioresorbable metal stent with controlled resorption due to a wrap with a special polymer, thereby ensuring a controlled resorption of the wrapped endoprosthesis subsequent to its implantation into a blood vessel. The resorbable implant comprises a magnesium alloy provided with a biodegradable coating. The biodegradable coating comprises biodegradable polymers and can further include at least one pharmacologically active substance such as an antiproliferative, antimigrative, antiangiogenic, antiinflammatory, antiphlogistic, cytostatic, cytotoxic and/or antithrombotic agent, anti-restenosis agents, corticoids, sex hormones, statins, epothilones, prostacyclins and/or inductors of angiogenesis.
CN103690576A High-seabuckthorn Vc sugar-free lozenge and preparation method thereof The invention belongs to the field of medicinal compositions, and in particular relates to a high-seabuckthorn Vc sugar-free lozenge and a preparation method thereof. The raw materials of the high-seabuckthorn Vc sugar-free lozenge comprise the following components in percentage by weight: 3.20-4.15% of seabuckthorn Vc dry powder used as a main material, 84.5-89.5% of sodium carboxymethylcellulose used as auxiliary materials, as well as 0.02-0.07% of sucralose, 2.93-4.18% of sorbic alcohol, 2.70-3.95% of sodium citrate, 1.65-3.15% of magnesium stearate and a freshener accounting for 0.002-0.003% of the total amount of the previous six raw materials, which are used as additives. The invention also provides the preparation method of the high-seabuckthorn Vc sugar-free lozenge, and the preparation method comprises the following steps: mixing the main material, the auxiliary material and seasonings with water, performing freeze-drying, vacuum microwave drying and granulation, and detecting indexes which are qualified to obtain a product. The lozenge prepared by the method disclosed by the invention is high in Vc content and provides a better choice for people requiring supplementation of Vc.
CN102872017A Use of 6-(4-difluoromethoxy)-3methoxyphenyl)pyridazine-3(2H)-one in preparation of antitumor drugs The invention relates to a use of 6-(4-difluoromethoxy)-3methoxyphenyl)pyridazine-3(2H)-one with the structure represented by formula I in preparation of antitumor drugs especially liver cancer resistant drugs.
US20120121687 Wound healing material and method for fabricating the same The present invention provides a wound healing material and method for fabricating the same. The wound healing material comprises a hydrophobic fluoro-containing membrane having a first surface and a second surface opposing to each other; and at least one biocompatible polymer covalently bonded to at least one part of the first surface of the membrane wherein the membrane is air permeable but liquid impermeable and the water contact angle of the first surface formed with the biocompatible polymer is smaller than or equal to 40 degrees.
US7001897 Such as (1R,5S,6S)-2-(1-(4-carbamoyl-1,3-thiazol-2-yl)azetidin-3-yl)thio-6-((1R)-1 -hydroxyethyl)-1-methylcarbapen -2-em-3-carboxylic acid for treatment/prevention of bacterial infections A 1-methylcarbapenem compound represented by the formula (I): having antibacterial activity, pharmacologically acceptable esters or salts thereof and pharmaceutical compositions (particularly antibacterial agents) containing them as an active ingredient are described. In addition, the invention includes the use of these compounds, ester derivatives or salts for the manufacture of pharmaceutical compositions, or a method for the prevention or treatment of diseases (particularly bacterial infections) by administering a pharmacologically effective amount of the compounds, ester derivatives or salts to warm-blooded animals (particularly human beings).
US20050158409 Beverage with proanthocyanidins; protecting blood vessels The composition of the present invention contains proanthocyanidins as active components. When the composition further comprises ascorbic acid or a derivative thereof, the fluidity of blood and effect of protecting blood vessels are further improved. This composition may be a food composition or pharmaceutical composition for improving the blood fluidity. Particularly, this composition is useful as a beverage.
CN101773517A H2S or H2S donator temperature sensitivity instant gel preparation for injection The invention discloses an H2S or H2S donator temperature sensitivity instant gel preparation for injection. The gel preparation is prepared from the following raw materials and auxiliary materials in mass volume ratio: 0.01%-10% of H2S or H2S donator, 17%-45% of instant gel substrate, 0.6%-5% of tackifier, 0.5%-2% of preservative, and 0%-10% of osmotic pressure regulator, wherein water or a buffer solution is solvent. The instant gel preparation for injection can effectively control the release speed of the H2S or the H2S donators in drugs and avoid untoward effect caused by abrupt release of H2S. After the gel preparation is injected, gel is formed at a local part and releases slowly, thereby reducing drug administration times, avoiding stimulation of penetrating odor of the H2S to patients, and being beneficial to the improvement of the biddability of patients.
US20120288573 Use of extracts from salonum glaucophyllum for treating bone metabolism disorders and kidney disorders A method is provided for preventing or treating bone or musculoskeletal metabolism disorders or kidney malfunction in humans. It comprises providing to a subject in need of that a calcium containing or calcium enriched diet combined with the administration of an efficient amount of a plant extract of Solatium glaucophyllum comprising from about 0.8 to about 2.2 weight % of a mixture of 1,25-dihydroxyvitamin D3 glycosides and quercetin glycosides present in a ratio of about 1:100 to 1:200 parts by weight. There are also provided food or dietary composition and food supplement designed for preventing or treating bone or musculoskeletal metabolism disorders or kidney malfunction in humans which comprises an efficient amount of the said plant extract of Solanum glaucophyllum and a source of calcium.
US20110150840 Detection and Treatment of Glyco-Enzyme-Related Disease The present invention relates to the prevention and treatment of a disease, preferably brain cancer, by administration of an isolated DNA molecule comprising a gene encoding a protein having glycosyltransferase activity to a cell involved in the disease which is preferably a glioblastoma cell. A method of treating brain cancer is provided in which a tumor cell is transfected either ex vivo or in vivo with a composition comprising a DNA molecule that encodes a protein having glycosyltransferase activity resulting in inhibition of the growth or function of that cell.
US20100197646 Solvent-based sterilisation of pharmaceuticals A sterile composition of a pharmaceutical compound is prepared by combining solvent with a non-sterile pharmaceutical compound to form a solution and filtering to yield a sterile pharmaceutical compound, optionally removing all or part of the solvent, and under sterile conditions combining the compound with a pharmaceutically acceptable carrier.
US20080268069 Mixture having effect of improving insulin resistance, effect of suppressing body weight gain, and effect of preventing and improving fatty liver The specification discloses a mixture obtained by mixing trivalent chromium and an onion extract, which has the effect of improving insulin resistance, suppressing body weight and preventing and improving fatty liver. Preferably the trivalent chromium is in a form of trivalent chromium-nicotinic acid complex.
EP1928450A2 Treating premature ejaculation using gabapentin and pregabalin prodrugs Disclosed herein is the use of prodrugs of gabapentin and pregabalin, and pharmaceutical compositions thereof, to treat premature ejaculation in male humans .
WO2012133960A1 Inhibitor for dipeptidyl peptidase iv The present invention relates to a substance for detecting the activity of dipeptidyl peptidase IV (hereinafter referred to as "DPPIV" or "DPP4") and suppressing a detected enzyme. The substance for inhibiting the DPP4 activity that is detected, according to the present invention, exhibits an excellent effect on inhibiting DPP4.
US20120021064 Compositions for bowel preparation and methods of use thereof The present invention relates to formulations and kits for gastrointestinal cleansing and to therapeutic methods thereof.
US20110003785 Fused Thiazole Derivatives As Kinase Inhibitors A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
CN1840172A Pidotimod solution capable of being administered from vein The invention provides a Pidotimod solution for intravenous injection, which comprise reactive compound of ((R)-3-[(S)-(5-oxo-2-pyrrolidinyl) carbonyl]-thiazolidine-4-carboxylic acid by a content of 0.4-200mg/ml, solvent for injection and solubilizing agent for injection, the solvent for injection comprises water, non-water solvent or their mixture.
US7307077 Heterocyclic compound and antitumor agent containing the same as effective ingredient The present invention relates to heterocyclic compounds represented by the formula I or pharmaceutically acceptable salts thereof and antitumor agents containing the heterocyclic compounds as effective components: wherein X represents nitrogen atom or CH; R1 represents CHnF3-n (wherein n is 1 or 2), hydroxy C1-C6 alkyl, NHR6 [wherein R6 represents hydrogen atom or COR (wherein R represents hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy)]; R2 represents morpholino (which may be substituted with one to four C1-C6 alkyl), thiomorpholino, piperidino, pyrrolidinyl (which may be substituted with hydroxy C1-C6 alkyl), oxazolidinyl (which may be substituted with one or two C1-C6 alkyl) or tetrahydro-1,4-thiazin-1-oxo-4-yl; R3 and R4 each represent hydrogen atom or C1-C6 alkyl; and R5 represents hydrogen atom, amino or hydroxyl.
CA2839264A1 Formulations of phospholipid comprising omega fatty acids Disclosed herein are stabilized powder and aqueous formulations comprising a phospholipid comprising omega fatty acid and a micelle-forming surfactant. In one embodiment, the formulation further comprises a water soluble reducing agent, and/or a metal chelator, and/or a metal bisulfite reducing agent, or combinations thereof, wherein the formulation remains substantially clear and stable when stored at or below room temperature for a period of at least 6 months or at least 12 months; and methods for preparing these formulations.
US20100136100 Removal promoters and inhibitor for apoptosis cells in vivo The present invention is to provide a removal promoter for apoptotic cells which is capable of immediately removing apoptotic cells in vivo by macrophages, or a removal inhibitor which inhibits the removal of apoptotic cells in vivo by macrophages. A removal promoter for apoptotic cells in vivo containing the milk fat globule-EGF factor 8-L (MFG-E8-L), MFG-E8-L mutant having removal promotion action for apoptotic cells in vivo by macrophages, or preferably a recombinant human or mouse MFG-E8-L, or a recombinant human or mouse MFG-E8-L mutant as an active ingredient is prepared. Such removal promoters specifically bind to apoptotic cells and promote the phagocytosis of apoptotic cells by macrophages by recognizing aminophospholipids such as phosphatidylserine exposed on apoptotic cell surface. On the other hand, a point mutation (D89E) MFG-E8-L mutant is used as a removal inhibitor.
CN103393594A Novel aripiprazole preparation composition The invention provides a novel aripiprazole preparation composition, and particularly relates to an oral administration drug solution composition which comprises 1.6-2.5mg/ml aripiprazole, an appropriate solvent system (water, a surfactant and a water-soluble thickening agent) and a pH stabilizing agent, wherein pH of a solution is 3.4 to 4.5. The drug solution composition is stable, and higher in drug loading capacity, and facilitates administration.
US20110166231 Method of treating a human being for a class of metabolic defects and energy production disorders The invention involves various embodiments of a method for treating a human being for a condition associated with (1) a clinical state of impairment of carnitine or carnitine esters, or decreased fatty acid metabolism, (2) low energy production or lower ATP production, (3) clinical hyperammonemia, and (4) clinically high pyruvate levels resulting from a deficiency in the biosynthesis of carnitine. The method involves administering a therapeutically effective salt of N-6-trimethyl-L-lysine.
US20110123631 Oral compositions of clindamycin A taste masked pharmaceutical composition of clindamycin, or a pharmaceutically acceptable salt(s), hydrate(s), solvate(s) and physiologically functional derivative(s) and precursors thereof, which includes all polymorphic forms, whether crystalline or amorphous comprising polyhydric alcohol(s); and one or more other pharmaceutically acceptable excipient(s). A process for preparation of a taste masked pharmaceutical composition of clindamycin or a pharmaceutically acceptable salt(s) thereof the said process comprising the steps of a) dry mixing clindamycin, polyhydric alcohol and other pharmaceutically acceptable excipient(s) to get a dry mixture; b) granulating the dry mixture above with a granulating liquid prepared by mixing the suitable pharmaceutically acceptable excipient(s) with aqueous/non-aqueous fluid to obtain a wet mass; c) drying the wet mass to obtain the discrete particles; d) lubricating the discrete particles obtained with a suitable lubricating agent and/or flavour(s).
EP2772522A1 Radical inhibitor A new radical inhibitor, a composition containing the new radical inhibitor, and a radical generation inhibition method using the new radical inhibitor are provided. A radical inhibitor according to the present invention contains a salen complex compound of a bivalent metal.
US20100273858 Compositions comprising stat5 sirna and methods of use thereof The present invention provides nucleic acid molecules that inhibit STAT5 expression. Methods of using the nucleic acid molecules are also provided.
US20090215880 Composition and Method for IN VIVO and IN VITRO Attenuation of Gene Expression Using Double Stranded RNA Introduction of double stranded RNA into cells, cell culture, organs and tissues, and whole organisms, particularly vertebrates, specifically attenuates gene expression.
CN102784069A Zinc-loaded calcium phosphate antibacterial material and preparation method thereof The invention relates to the field of an antibacterial material, in particular to a zinc-loaded calcium phosphate antibacterial material and a preparation method of the zinc-loaded calcium phosphate antibacterial material. The preparation method of the zinc-loaded calcium phosphate antibacterial material is as follows: 1) carrying out coprecipitation reaction to obtain calcium phosphate; 2) dissolving zinc salt into an organic solvent to obtain a zinc salt saturated solution, wherein the zinc salt is water soluble zinc salt, and the organic solvent is organic solvent which is mutually soluble with water; 3) adding the calcium phosphate prepared in the step 1) into the zinc salt saturated solution prepared in the step 2), and stirring or ultrasonically oscillating to obtain white precipitate; and 4) separating, washing and drying the white precipitate in the step 3) to obtain the zinc-loaded calcium phosphate antibacterial material. The zinc-loaded calcium phosphate antibacterial material provided by the invention is high in zinc-loaded content and has a dual antibacterial mechanism of Zn <2+> antibacterial effect and antibacterial effect of a zinc-containing compound; and the preparation method has the advantages of simple technology, rapidness, low cost, low biotoxicity and environmental friendness and the like.
CN102920710A Medicinal composition of cefodizime compound A medicinal composition of a cefodizime compound comprises cefodizime crystals and sodium carbonate, wherein the weight percentage of cefodizime crystals and sodium carbonate is 100:8-100:11, a diffraction pattern of an X-ray powder of the cefodizime crystal is shown in figure 1, wherein 2 theta is displayed with the characteristic peaks at 6.58 degrees +/-0.1 degrees, 11.22 degrees+/-0.1 degrees, 11.51 degrees +/-0.1 degrees, 15.82 degrees+/-0.1 degrees, 16.52 degrees+/-0.1 degrees, 17.21 degrees +/-0.1 degrees, 19.49 degrees+/-0.1 degrees, and 23.04 degrees+/-0.1 degrees, and the water solubility of the composition is improved; when the composition and the anhydrous sodium carbonate are prepared into sterile powder injection, the dose of the anhydrous sodium carbonate is greatly reduced, and the dissolving speed is fast, namely the composition is completely dissolved in a short time, and the stability is good, so that the medicinal composition of the cefodizime compound is convenient for clinical use.
WO2007011720A2 Cyclopentane n-lower alkyl heptenamide-5-cis-2- (3alapha- hydroxy-5-phenylpentyl) -3, ?5-dihydroxy, [1alpha, 2beta, 3alpha, 5alpha] compounds as agents for lowering intraocular pressure The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein R is a lower alkyl radical, i.e. a C1-C6 alkyl radical, e.g. a methyl, ethyl or propyl radical. Most preferably said compound is (Z)-7-[lR, 2R, 2R, 5S)-3,5-Dihydroxy-2-[lE, 3S)-3-hydroxy-5-phenyl-l-pentyl]cyclopentyl]-5-N-ethylheptanamide.
WO2010087577A3 Use of thymus capitatus extract, satureja hortensis extract, or carvacrol for treating metabolic diseases The present invention relates to the use of Thymus capitatus extract, Satureja hortensis extract, or carvacrol for treating metabolic diseases. More specifically, the present invention relates to a composition, use thereof, and a method using the same. The composition contains as active ingredient, extract of Thymus capitatus, extract of Satureja hortensis or carvacrol, which is an aromatic oil commonly found in mint, oregano, thyme, bergamot, camphor or thymol, for preventing and treating a metabolic disease selected from the group consisting of obesity, fatty liver, hyperlipidemia and diabetes. The composition, use and method of the present invention are useful for weight loss, suppression of intra-abdominal fat accumulation, and treatment of fatty liver. Also, the composition, use, and method remarkably reduce cholesterol and free fatty acid content in plasma and liver tissue, blood glucose and insulin resistance.
US20110136910 Method for stabilization of s-nitrosoglutathione and composition prepared by the same The invention relates to pharmaceutical compositions having alkaline pH comprising S-nitrosoglutathione (GSNO) as active ingredient together with usual additives, optionally with one or more polysaccharide-type polymer(s). Another subject of the invention is a method for stabilizing a solution or non-solid composition containing GSNO wherein the pH of the solution or composition is adjusted to an alkaline value.
US6936718 Reacting with acid mixed with solvent; salt formation In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of specific, preferred rotamer or rotameric pair of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing desired rotamers of pharmaceutically useful salts.
WO2014158875A1 Novel therapy for prostate carcinoma Disclosed herein are methods of inhibiting or delaying the growth of androgen-dependent prostate cancer, and/or inhibiting or delaying the onset of castration-resistant prostate cancer (CRPC) by administering naphthoquinone analogs, such as plumbagin, and specified hormone therapy agents, including selective inhibitors of 17,20-lyase activity of CYP 17.
CN103622966A Application of tozasertib in preparation of drugs for treating schizophrenia The invention discloses a novel application of tozasertib and analogues compounds of tozasertib or pharmaceutical salts of tozasertib, and the novel application is an application in preparation of drugs for treating schizophrenia. The tozasertib and analogues compounds of tozasertib or pharmaceutical salts of tozasertib can be made into normal preparations and long-acting preparations. The preparations mentioned above have a prominent effect on schizophrenia treatments and do not have any side or toxic effect.
CN1593422A Method for preparing freeze dried cefathiamidine The invention provides a method for preparing freeze dried cefathiamidine which comprises the steps of, dissolving the purified crude product of cefathiamidine with water, adjusting pH to be 4.0-6.0, filtering, washing with slight amount of water, cooling the solution to -60 - -20 deg. C for solidifying, then slowly elevating temperature to 0-60 deg. C under high vacuum so as to gasify the moisture, and strictly controlling the freeze-drying curves.
US20080027050 Heterocyclic Amide Compound and Use Thereof as an Mmp-13 Inhibitor(Amended Ex Officio) The present invention provides a novel amide derivative having a matrix metalloproteinase inhibitory activity, and useful as a pharmaceutical agent, which is a compound represented by the formula (I) wherein ring A is an optionally substituted, nitrogen-containing heterocycle, ring B is an optionally substituted monocyclic homocycle or an optionally substituted monocyclic heterocycle, Z is N or NR1 (R1 is a hydrogen atom or an optionally substituted hydrocarbon group), is a single bond or a double bond, R2 is a hydrogen atom or an optionally substituted hydrocarbon group, X is an optionally substituted spacer having 1 to 6 atoms, ring C is (1) an optionally substituted homocycle or (2) an optionally substituted heterocycle other than a ring represented by (II) (X′ is S, O, SO, or CH2), and at least one of ring B and ring C has substituent(s), provided that N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl}-5,6-dimethyl-4-oxo-1,4-dihadrothieno[2,3-d]pyrimidine-2-carboxamide is excluded, or a salt thereof.
US20100093678 Compositions and methods of the treatment of obesity and osteoporosis The present invention relates to naturally occurring compositions comprising vitamin D3 or related analog and methods for treating obesity and/or osteoporosis and reducing body fat or enhancing a bone graft in patients in need thereof.
EP1603912A1 Substituted piperidine and piperazine derivatives as melanocortin-4 receptor modulators The present invention relates to novel substituted piperidine and piperazine derivatives as melanocortin-4 receptor (MC-4R) modulators. MC-4R agonists of the invention can be used for the treatment of disorders and diseases such as obesity, diabetes, and sexual dysfunction, whereas the MC-4R antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. All diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
CN102603836A Schisandrin C simplifier, schisandrin analogue, preparation method and applications thereof The invention discloses a schisandrin C simplifier, a schisandrin C analogue, a preparation method and applications of the schisandrin C simplifier and the schisandrin C analogue, and relates to pyrimidine nucleoside derivatives formed by seven-position substitution of biphenyl compounds, a preparation method of the pyrimidine nucleoside derivatives and applications of the pyrimidine nucleoside derivatives in antiviral aspect, belonging to the field of pharmaceutical chemistry. The schisandrin C simplifier and the schisandrin analogue have the following general structure formula shown as the pictures in the abstract, wherein BR1=CH3, C2H5, i-C3H7; when R2=CH3, R3+R4=-CH2-; and when R4=CH3, R2+R3=-CH2-. The compounds have the activities of antiviral, resistance to infection and proliferation and the like, is feasible in the preparation method, is applied to medicaments for treating virus and has good application prospect.
CN1850111A Biodegradeable hemostasis powder The present invention relates to a hemostatic powder which has high swelling rate and can be bio-degradable. It is made up by using carboxymethl chitosan, sodium alginate and calcium chloride as main raw material, through a certain preparation process.
US20060270692 2-(4-{[7-(3-chloropropoxy)-6-methoxyquinazolin-4-yl]amino}-1H-pyrazol-1-yl)-N-(3-fluorophenyl)acetamide; colorectal cancer Quinazoline derivatives of formula (I); for use in the treatment of proliferative diseases such as cancer and in the preparation of medicaments for use in the treatment of proliferative diseases, and to process for their preparation, as well as pharmaceutical compositions containing them as active ingredient.
CN102247313A Oral-administration slow release solid preparation by taking Moxifloxacin as active ingredient The invention relates to an oral-administration slow release solid preparation by taking Moxifloxacin as an active ingredient. The oral-administration slow release solid preparation is prepared from Moxifloxacin, the salt thereof and pharmaceutically acceptable auxiliary materials by the preparation technology. The oral-administration slow release solid preparation disclosed by the invention not only comprises tablets, capsules, particles and slow release pillets. The oral-administration slow release solid preparation has stable and controllable quality and is safe and effective.
US20070155966 Heterocyclic imines such as 2,2-Dichloro-N-[2-[3-(2-chloro-6-fluorophenyl)-5-isoxazolyl]-(4-pyridyl)]Acetamide, used for prophylaxis of hepatitis C virus (HCV) The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles and hydro isomers thereof and/or pharmaceutical compositions comprising the compounds to treat or prevent HCV infections
CN102100676A Vinpocetine orally disintegrating tablets The invention discloses vinpocetine orally disintegrating tablets and a preparation method thereof. The main medicament of the orally disintegrating tablets is vinpocetine; and the auxiliary materials comprise microcrystalline cellulose, mannitol, lactose, cross-linked polyvinyl pyrrolidone, sodium cyclamate, menthol, aerosil and magnesium stearate. The vinpocetine orally disintegrating tablets can effectively treat senile dementia, particularly vascular senile dementia, are conveniently taken, has good mouthfeel, quick disintegration, quick absorption and high bioavailability, and provides convenience for senile dementia patients inconvenient to take medicaments.
CN102727529A Radical treatment soup for Aids The invention relates to a medicament for treating aids, the medicament is prepared by mixing an organic matter and a medicinal mineral. The aim of the invention is reached by the following steps: the medicament is prepared by the following raw materials, by weight part, toad one part and liqueur five parts. According to the invention, insufficient of the present technology is overcome, and the medicament provided in the invention has the advantages of simultaneous treatment of principal and subordinate symptoms, no pain in treatment, rapid drug effect and radical treatment.
WO2013161308A1 Amide derivatives as ttx-s blockers The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
CN102133175A Amygdalin gel and preparation method and medicinal application thereof The invention discloses amygdalin gel and a preparation method and medicinal application thereof, belonging to medicinal preparations containing organic active components. The preparation method comprises the following steps of: adding distilled water to 1-15% of amygdalin as a medicinal material till dissolution; adding 0.5-10% of a high polymer host material carbomer for fully swelling; then respectively adding 1-25% of glycerol as a humectant, 0.5-20% of propylene glycol as a penetrating agent, 0.05-0.2per mill of ethyl p-hydroxybenzoate as a preservative and 0.01-0.2% of disodium ethylene diamine tetraacetate as a stabilizer; regulating the pH to 6.0-8.0 by 0.5-3% of triethanolamine; finally adding distilled water to 100%; and fully stirring to form gel. The amygdalin gel prepared by the preparation method has no irritation and allergization on skin, can release the medicament stably and persistently, and has high bioavailability and satisfactory percutaneous infiltration rate, so that the amygdalin gel becomes a new external medicinal preparation.
WO2012128496A3 Pharmaceutical composition for preventing or treating asthma containing maackiain as an active ingredient The present invention relates to a pharmaceutical composition for preventing or treating asthma containing maackiain as an active ingredient. The maackiain of the present invention can be used to advantage as a composition for preventing, treating and alleviating asthma because it has an outstanding effect in suppressing the production of ovalbumin and in particular IgE in serum and bronchoalveolar lavage fluid and in suppressing the expression of Th2 cytokines in the lungs, in addition to suppressing the volume of active oxygen created in the respiratory tract and suppressing the infiltration of inflammatory cells into the bronchi and relieving respiratory-tract hypersensitivity which constitute problems that cause asthma in in-vivo studies.
WO2014138824A1 Immune modulation The present invention relates to a poxvirus vector comprising a nucleic acid sequence encoding a fusion protein comprising: (i) a peanut allergen selected from list consisting of at least two peanut allergens from ara h 1, ara h 2, ara h 3, ara h 4, ara h 5, ara h 6. ara h 7, ara h 8, ara h 9, ara h l O and ara h I I or a derivative or part thereof having at least 70% sequence identity thereto, and (ii) a profeasome degradation tag to enhance intracellular degradation of the fusion protein. Methods of desensitizing or inducing tolerance to a peanut allergen and/or suppressing an allergic response to a peanut allergen are also disclosed.
CN103285406A MicroRNA-203, and application of analogue thereof in preparation of medicament for preventing and treating obesity, dyslipidemia and complication of obesity and dyslipidemia The invention discloses microRNA-203, and application of an analogue of the microRNA-203 in preparation of a medicament for preventing and treating obesity, dyslipidemia and complication of the obesity and the dyslipidemia and belongs to the field of biological medicine. The prepared medicament disclosed by the invention can be miR-203 and a single ingredient of the analogue of the miR-203, and also can be a pharmaceutical composition. The pharmaceutical composition is prepared from effective dosage of miR-203 and/or analogue thereof and a pharmaceutical acceptable carrier in a mixing manner; the carrier can be cholesterol, virus, nano-particles, chitosan, lipidosome and the like; synthetic miR-203 and/or the analogue thereof are/is connected with the carrier to form the medicament. The medicament can be used for treating the obesity, the dyslipidemia or the complication of the obesity and the dyslipidemia by vein, muscle or intraperitoneal injection and the like.
US20120244095 Compositions containing polymeric, ionic compounds comprising imidazolium groups The present invention relates to compositions containing polymeric, ionic compounds comprising imidazolium groups. In particular, it relates to the use of polymeric, ionic compounds comprising imidazolium groups in personal care compositions and/or in biocide compositions.
CN103127504A Compositions and methods for topical nitric oxide generation A simple, biocompatible two-component system and procedure for generating nitric oxide (NO) is described. One component comprises sodium nitrite or other nitrite source, and the other component comprises a reductant, an acid and a base although in certain embodiments the reductant and acid functions are provided by the same component. When these two components are mixed directly at a local site of administration or immediately prior to application and the mixture generates nitric oxide (NO) for topical application. The activated system is therapeutic for treatment of multiple conditions, including promotion of healing, disinfection, promotion of hair growth, and treatment of male and female sexual dysfunction.
US20050261344 Treatment of lower urinary tract symptoms associated with overactive bladder in men and women This invention relates to pharmaceutical combinations suitable for treating the lower urinary tract symptoms associated with either overactive bladder or mild to moderate benign prostatic hyperplasia, which combinations contain an alpha-adrenoceptor antagonist and a 5-HT4 antagonist. The combinations of the invention are particularly suitable for treating moderate or severe symptomatology.
US7507758 4-alkyl-/4-alkenyl-/4-alkynyl methyl/-1-aryl-cyclohexylamine compounds 4-alkyl/4-alkenyl/4-alkynyl methyl/-1-arylcyclohexylamine compounds corresponding to the formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them to treat or inhibit pain or other specified conditions associated with the ORL1 receptor.
WO2008006043A2 1,3-oxazole derivatives useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic and anti-obesity agents Compounds are provided which have the structure of Formula (I): wherein R1 is halogen; and X is hydrogen or halogen, and salts thereof, which compounds are useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic, and anti-obesity agents.
CN102362877A Pouzolzia extract, preparation method thereof, and application thereof The invention discloses a pouzolzia extract, a preparation method thereof, and an application thereof. According to the invention, for a first time, four compounds are separated and identified from subsiding swelling and pus removing effective parts of pouzolzia. A water extract prepared from pouzolzia and a chloroform or n-butyl alcohol extracted part thereof provide subsiding swelling and pus removing effects. The chloroform extracted part contains friedelin. The n-butyl alcohol extracted part contains kaempferol-7-O-alpha-L-pyran rhamnoside, quercetin-7-O-alpha-L-pyran rhamnoside, quercetin-3, and 7-O-alpha-L-2-pyran rhamnoside. The extract provided by the invention provides good subsiding swelling, pus removing, inflammation resisting, and pain relieving effects. The extract can be used for preparing subsiding swelling and pus removing medicines.
CN103202837A Applications of artemisine derivatives and pharmaceutically acceptable salts thereof in preparing drugs for treating leukemia The invention discloses applications of artemisine derivatives and pharmaceutically acceptable salts thereof. The artemisine derivative-arteether dimer amine and the pharmaceutically acceptable salts thereof can inhibit the proliferation of leukemic cells and induce the apoptosis of tumor cells. The artemisine derivative-arteether dimer amine and the pharmaceutical salts thereof provided by the invention can be applied in preparing drugs for treating leukemia, especially in preparing drugs for treating acute leukemia, more especially in preparing drugs for treating acute myelocytic leukemia, and particularly in preparing drugs for treating M3 subtype acute myelocytic leukemia.
CN102038663B Carbazole sulfonamide antineoplastic agent capsules and preparation method The invention belongs to the field of pharmaceutic preparations and relates to a preparation method of the antineoplastic agent, in particular to carbazole sulfonamide antineoplastic agent capsules and a preparation method thereof. The carbazole sulfonamide antineoplastic agent capsules are characterized in that: lactose and beta-cyclodextrin are added into a carbazole sulfonamide medicine, namely N-(2,6-dimethypyridine-3-yl)-9-methylcarbazole-3-sulfamide; the materials are mixed and ground into micro powder; the micro powder is granulated, and the granulates are formed into capsules; and thedissolution rate of the capsules are improved.
US20080214613 Substituted benzimidazole compounds with dual NOS inhibitory activity and mu opioid agonist activity The present invention relates to benzimidazole compounds having dual nitric oxide synthase (NOS) inhibitory activity and agonist activity at the mu-opioid receptor, to pharmaceutical and diagnostic compositions containing them, and to their medical use, particularly as compounds for the treatment or prevention of chronic pain, acute pain, migraine, and neuropathic pain.
CN103156857A Ceftezole sodium pharmaceutical composition powder injection The invention provides a ceftezole sodium pharmaceutical composition powder injection and relates to the field of pharmaceutical preparations and a preparation method thereof. The ceftezole sodium pharmaceutical composition powder injection mainly solves the problem that the existing ceftezole sodium and metronidazole single-component preparations have large use amounts, and have poor effects and side effects after combination. The ceftezole sodium pharmaceutical composition comprises ceftezole sodium and metronidazole lipid microspheres, wherein based on metronidazole weight, a weight ratio of the ceftezole sodium to the metronidazole lipid microspheres is in a range of (100: 4) to (100: 15). The ceftezole sodium pharmaceutical composition is processed into the ceftezole sodium pharmaceutical composition powder injection. An aqueous solution of the ceftezole sodium pharmaceutical composition has a pH value of 4.5-6.5. The ceftezole sodium pharmaceutical composition powder injection has high curative effects and reduces a metronidazole use amount by above 80% so that metronidazole toxic and side effects especially on the digestive tract such as nausea, vomit, inappetence, abdominal cramp and neurotoxicity are greatly reduced and an adverse reaction occurrence rate is reduced.
CN101543476B A naringin solid dispersion and the preparation method, and the application thereof The invention discloses a naringin solid dispersion, and the preparation method and the application thereof. The naringin solid dispersion contains naringin and vector material. The mass ratio of naringin and the vector material is 1:2 to 1:5. The vector material is any one of or any mixture of polyethylene glycol, polyvinyl pyrrolidone and poloxamer. The preparation method of the naringin solid dispersion is to get the naringin, the vector material and the other regular auxiliary materials by melting method, solvent method, solvent-melting method, spray drying method or freeze-drying method.The application of the naringin solid dispersion is to apply in preparing pharmaceutical preparations or healthfood. The invention of the naringin solid dispersion is to disperse naringin by solid dispersion technique, which improves the solubility in water and dissolution rate in vitro and at the same time enhances the bioavailability.
EP1027058B1 Disaccharide derivatives for treating hyperglycaemia The invention relates to the use of the disaccharide derivatives 3'-aminosaccharose, saccharose-C6-acid and palatinose-C6'-acid and/or an amide or alkylester thereof for preventing or treating hyperglycaemia.
US20100152298 Present invention relates to a treatment for the management of cancer more specially the use of Flutamide anti-androgen drugsa This invention helps in the treatment and the management of cancer. It is the use of flutamide drug to treat and manage cancer where the Flutamide anti-androgen drug acts in another mechanism other than the well know androgen respects (AR) mechanism.
CN103402530A Compositions and methods for treating erectile dysfunction Compositions for treating erectile dysfunction ("ED"), including age related erectile dysfunction (ARED), comprise in a preferred embodiment ginger and an amino acid. Preferably the amino acid is L-arginine and/or L-citrulline. Additionally, the compositions may comprise guarana (Paullinia cupana), Muira puama cortex magnoliae officinalis (CMO) and/or fructus aurantil immaturus (FAI). A daily dosage of at least about 250 mg ginger (or ginger derivative) and at least about 400 mg L-citrulline or L-arginine (or a mixture of L- citrulline and L-arginine) for a sufficient period of time (e.g., at least 30 days) will result in improved IIEF scores in a substantial number of patients that are experiencing ED or ARED and/or will result in maintenance of IIEF scores for patients that might otherwise experienced a decrease in IIEF scrores.
CN102357096A Statins zinc salt-containing blood fat-reducing composite The invention relates to an oral drug composite for reducing the blood fat, in particular to a drug composite which takes any 1-2 of statins zinc salt and nicotinic acidniacin blood fat reducing medicine or fibrates blood fat reducing medicine or cholesterol restraining and absorbing medicine as active ingredients, the preparation of the drug composite, and the use of the drug composite. The drug composite takes the statins zinc salt and the nicotinic acidniacin blood fat reducing medicine or the fibrates blood fat reducing medicine or the cholesterol restraining and absorbing medicine as the active ingredients and takes the corresponding ingredients as the drug auxiliary materials. The oral preparation which is prepared according to the technology and the method of the patent description comprises granular formulation, conventional tablet, chewable tablet, dispersible tablet, orally disintegrating tablet, buccal tablet, capsule, soft capsule, pill, sustained release tablet, sustained release capsule and the like. The oral drug composite is quick and durable in effect, and is convenient to take, thereby being used for treating various hyperlipemias.
WO2007144668A3 Process for the preparation of s-fluoromethyl-6, 9 -difluoro-11 -hydroxy-16 -methyl-17-propionyloxy-3-oxo-androsta-1,4-diene-17 -carbothioate and intermediates The present invention relates to a process for the preparation of steroidal 17β-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17β-carboxylic thioates, such as fluticasone propionate formula (I), using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds formula (II) resulting in selective and controlled fluorination. The present invention also relates to intermediates formula (II) and their preparation.
US7531162 Transcobalamin receptor binding conjugates useful for treating abnormal cellular proliferation An agent, composition and method for the treatment, prophylaxis and/or diagnosis of proliferative disorders, which is highly and efficiently absorbed at the site of abnormal cellular proliferation is disclosed.
WO2007007886A1 An oxime derivative and preparations thereof The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.
WO2013168826A1 Method for screening for prophylactic or therapeutic agent for diseases or disorders associated with inflammation-related feedback loop The purpose of the present invention is to elucidate a regulation molecule or a target molecule for an IL-6 amplifier, and provide a method for screening for a prophylactic or therapeutic agent for diseased or disease conditions of which the onset and/or worsening is induced through the activation of an IL-6 amplifier. A specific gene which can potentially regulate the onset or worsening of diseases or disease conditions in human through the activation of an IL-6 amplifier is identified, and it is found that the gene or a product of the gene can become a target for the prevention or treatment of diseases or disease conditions associated with the activation of an IL-6 amplifier including autoimmune diseases. This finding leads to the accomplishment of the screening method of the present invention.
CA2439408C Use of natural egfr inhibitors to prevent side effects due to retinoid therapy, soaps, and other stimuli that activate the epidermal growth factor receptor Many human conditions, often skin conditions, are treated topically or orally with a retinoid such as retinoic acid or acetretin, which treatment often has the side effect of dry, irritated, and/or peeling skin. The use of soaps, detergents, chemical irritants, and such can also cause these same side effects. These side effects can be reduced or eliminated by the topical administration of an inhibitor, especially a natural inhibitor, of the epidermal growth factor receptor (EGFR), administered concomitantly with the retinoid, separately from the retinoid (such as on an as-needed basis), or both. Administration of the two together is facilitated by a composition suitable for topical application and comprising both retinoid and a natural EGFR inhibitor. Preferred natural inhibitors are genistein and other isoflavones extracted from natural occurring substances, or simple derivatives of such substances.
CN102309451A Nifuratel liposome solid preparation The invention discloses a nifuratel liposome solid preparation and its preparation method, which is characterized in that the solid preparation comprises the following components by weight: 100 parts of nifuratel, 100-300 parts of sphingomyelin, 100-300 parts of egg phosphatidylcholine, 50-100 parts of cholesterol, 50-200 parts of tween 40, 10-20 parts of vitamin E and 75-150 parts of other pharmaceutical common auxiliary materials. The invention employs an anti-phase evaporation method for preparing nifuratel liposome solid which substantially raises the biological availability and stability of nifuratel, raises the product quality of the preparation, minimizes the toxicity and side effect, enhances the curative effect and greatly serves for the clinical application.
CN103222983A Use of peracetylated chitooligosaccharide in preparing drug for treating neurodegenerative disease The invention provides a use of peracetylated chitooligosaccharide in preparing a drug for treating neurodegenerative disease. According to the experiments, the peracetylated chitooligosaccharide has a protective effect to PC-12 cell injury induced by glutamic acid, and can be used for effectively lowering accumulation of reactive oxidative species (ROS) and reducing the release of lactic dehydrogenase (LDH). Moreover, the peracetylated chitooligosaccharide further can be used for remarkably improving mitochondrial transmerabrane potential and restraining a cell apoptosis way to achieve the protective effect to nerve cells. The peracetylated chitooligosaccharide provided by the invention has the advantages of being simple in preparation, specific in structure, higher in purity and the like. According to the in-vitro experiment, the peracetylated chitooligosaccharide has good nerve cell protective activity which indicates that the peracetylated chitooligosaccharide can be developed into a neuroprotective agent for treating the neurodegenerative disease.
US20080206362 Bathtub with carbon dioxide gas nanobubble-producing section therein In order to provide a device and a method for increasing blood flow and an insulin-like growth factor with use of a large amount of carbonic gas nano bubbles, the device of the present invention includes: a bathtub 1; and a nano bubble-producing section 41 for producing carbonic gas nano bubbles in bath water in the bathtub 1.
US7026484 For therapy of cancer This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.
CN101336723A Health food for relieving physical fatigue The invention discloses a health food for alleviating fatigue, which is composed of following active ingredients by weight: 15-75% of L-arginine, 10-70% of taurine, 0.1-20% of nutrient selenium, and 10-70% of nutrient zinc, in which L-arginine produces NO, taurine effectively restrains the consumption of oxygen, nutrient selenium eliminates free radicals, and nutrient zinc alleviates the injury to the body. The health food is produced by mixing the active ingredients in weight proportion according to the function thereof respectively, which can give full play to the role of alleviating fatigue. It is proven by the animal test that the health food has the function of alleviating fatigue.
WO2008035207A3 2-methylene-1alpha-hydroxy-19,21-dinorvitamin d3 analogs and uses thereof Compounds of formula I are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
WO2012113850A2 (PYRIDIN-4-YL)BENZYLAMIDES AS ALLOSTERIC MODULATORS OF ALPHA 7 nAChR The present invention relates to (pyridin-4-yl)benzylamides derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists.
EP1499353A2 Antibodies that specifically bind to tl5 The present invention relates to antibodies and related molecules that specifically bind to TL5. Such antibodies have uses, for example, in the prevention and treatment of cancer as well as immune system diseases and disorders including autoimmune disease, rheumatoid arthritis, graft rejection, graft vs. host disease, and lymphadenopathy. The invention also relates to nucleic acid molecules encoding antiTL5 antibodies, vectors and host cells containing these nucleic acids, and methods for producing the same. The present invention relates to methods and compositions for preventing, detecting, diagnosing, treating or ameliorating a disease or disorder, especially cancer as well as immune system diseases and disorders including autoimmune disease, rheumatoid arthritis, graft rejection, graft vs. host disease, and lymphadenopathy, comprising administering to an animal, preferably a human, an effective amount of one or more antibodies or fragments or variants thereof, or related molecules, that specifically bind to TL5.
CN102309443A Small cluster water zinc supplementation oral liquid, and preparation method and application thereof The invention discloses a small cluster water zinc supplementation oral liquid, and a preparation method and application thereof. The small cluster water zinc supplementation oral liquid comprises ingredients of zinc medicament, methylpyridine acid, sweetener and edible essence. The invention combines a characteristic that small cluster water can be easily absorbed by cells and a characteristic that methylpyridine acid can promote zinc absorption with zinc supplementation; water molecule cluster is treated into small clusters and coordinated with zinc to form zinc coordinated water, which haszinc as a center and 6-8 surrounding water molecules; and the obtained small cluster water zinc supplementation oral liquid has a higher absorptivity than an ordinary zinc oral liquid.
CN103751156A Piceatannol-containing composition, and drinking food and cosmetics containing piceatannol-containing composition A purpose of the present invention is to provide a high piceatannol content piceatannol-containing composition derived from natural materials, and a preparation method thereof. According to the present invention, the piceatannol-containing composition containing 0.0001-99.9% by mass of piceatannol is extracted from passion fruit seeds; and during extraction of the piceatannol, after the passion fruit seeds are crushed, at least a solvent selected from a water-containing alcohol solvent or a water-containing ketone solvent is added to stir, the piceatannol is extracted from the passion fruit seeds contained in the solvent, and stage extraction is performed by preferentially using the two solvents such as the water-containing alcohol solvent and the water-containing ketone solvent.
US20120252837 Bicyclic derivatives of azabicyclic carboxamides, preparation thereof and therapeutic use thereof The disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, Y, n, A, and W are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for the preparation of these compounds and the therapeutic use thereof.
CN102861340A Intelligent nano delivery system, preparation method and application thereof The invention discloses an intelligent nanoparticle drug release system capable of delivering biomacromolecules and small organic molecules to cells, a preparation method of the intelligent nanoparticle drug release system, and application of the intelligent nanoparticle drug delivery system in cell delivering of biomacromolecules and small organic molecules (including drugs). By delivering biochemical substances of drug molecules, cell nutrients and cell expellant, physiological metabolism and pathological metabolism are intervened. Molecule delivery of an embodiment of the intelligent nanoparticle drug delivery system includes but is not limited to the following molecules: telomerase cell delivery; antioxidant enzyme (such as SOD (superoxide dismutase) and HPX (hydrogen peroxidase)) cell delivery; cancer suppressor protein (such as p53 and PTEN(phosphatase and tensin homolog deleted on chromosome ten)) cell delivery; and organic chemical and biochemical small molecules (such as atorvastatin-lipitor and coenzyme Q-10) cell delivery. The molecule slow release and control of the nanoparticle drug delivery system has uniqueness and targeting so that the nanoparticle drug delivery system is intelligent.
EP1708712A1 Treatment of malignant gliomas with tgf-beta inhibitors The invention concerns methods of treating malignant gliomas, by administering inhibitors of TGF-β the TGF-β signaling pathway, including molecules preferably binding to the type I TGF-β receptor (TGFβ-R1). Preferably, the inhibitors are non-peptide small molecules, including quinazoline derivatives. The invention also concerns methods for reversing the TGF-β-mediated effect on glioma cells to make them less refractile to signaling and other immune cells, comprising contacting a glioma cell or tissue in vivo or in vitro, with an inhibitor of TGF-β.
US20050159329 Low reducing sugar content, high level of alpha glucoside bonds, narrow range of high molecular weights, specific branched chain length distribution profile; low intrinsic viscosity; food, and medical applications The invention relates to soluble highly branched glucose polymers, having a reducing sugar content of less than 1%, a level of α-1,6 glucoside bonds of between 13 and 17% and an Mw having a value of between 0.9×105 and 1.5×105 daltons, characterized in that their branched chain length distribution profile consists of 70 to 85% of DP of less than 15, of 10 to 16% of DP of between 15 and 25 and of 8 to 13% of DP greater than 25.
CN101057846A Lansoprazole for injecting and its preparation method The invention discloses a Lansoprazole preparation for injection comprising (1) Lansoprazole 10-50 weigh parts, (2) meglumine 2-20 weight parts, (3) sodium hydroxide 1-5 weight parts, (4) mannitol 20-100 weight parts. The invention also discloses the process for preparing the preparation.
CN102229877A Brewing method for pine pollen wine The invention relates to a brewing method for pine pollen wine. In the prior art, the brewing method for the pine pollen wine has not characteristics of simple production process, low brewing cost and good efficacy of the prepared pine pollen wine. The brewing method provided by the present invention is characterized in that: raw materials of the pine pollen wine comprise: 48.0 g of broken pine pollen, 16.0 g of medlar, 24.0 g of tuckahoe, 18.0 g of mycelium of cultured cordyceps sinensis, 1.6 g of taurine, sorghum wine having a volume percent concentration of 50% and water. The method sequentially comprises processes of immersing, blending, filtering and filling. During the dipping process and the blending process, the broken pine pollen, the medlar, the tuckahoe, the mycelium of cultured cordyceps sinensis and the taurine are placed in a immersion tank, followed by adding the sorghum wine and immersing for 20-30 days to obtain supernatant; the supernatant is filtered through a pressure filtration to obtain filtrate, followed by adding water to blend the filtrate to a volume percent of 36%. During the filtering process, the filtrate from the dipping process and the blending process is filtered again to obtain the secondary filtrate, followed by standing for 48 hours to obtain half-finished product wine. The method provided by the present invention has advantages of simple production process, low brewing cost and good efficacy of the prepared pine pollen wine.
WO2004064717A3 Cop 1 for treatment of inflammatory bowel diseases The present invention relates to the use of Copolymer 1 (glatiramer acetate), a Copolymer 1-related polypeptide, or a Copolymer 1-related peptide, for the treatment of inflammatory bowel diseases such as Crohn's disease and ulcerative colitis.
US20100298302 Novel protein kinase modulators The invention provides compounds that inhibit selected kinases (Pim, Flt and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders.
US7074930 Amine salts of an integrin receptor antagonist Amine salts of 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3-(6-methoxy-pyridin-3-yl)propionic acid are potent antagonists of the integrin αvβ3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts.
WO2014154179A1 2β,3α,5α-TRIHYDROXY-ANDROST-6-ONE AND PREPARATION METHODS AND USE THEREOF The present invention discloses compound 2β,3α,5α-trihydroxy-androst-6-one, having the structure of formula (I). The present invention also discloses a plurality of methods for preparing the compound and a use of the compound.
CN102219768A Perylenequinone compounds and their extraction and separation method and use The invention discloses novel perylenequinone compounds. The novel perylenequinone compounds have respectively structural general formulas of I to VI. The perylenequinone compounds are isolated from fermentation liquor of endophytic fungi (Phaeosphaeria sp.) of physcia lichens. Purities of the perylenequinone compounds are over 98%. A result of an antibacterial activity experiment shows that someof the perylenequinone compounds have good antimycotic effects. A result of an antineoplastic activity experiment shows that the perylenequinone compounds have good antineoplastic effects. The perylenequinone compounds have obvious effects of killing tumor cells under an illumination condition. Under the condition of severe drug resistance, the perylenequinone compounds of I to VI have good exploitation, utilization and development prospects, can be utilized as lead compounds for research and development of antimycotic and antineoplastic drugs and provide a novel approach for the research andthe development.
US20080064678 N-tert-Butyl-2-[3-(4-fluoro-3-methoxyphenyl)-1-oxo-7-(3-pyrrolidin-1-ylpropoxy)-1H-isoquinolin-2-yl]acetamide; 2-[3-(3-Chlorophenyl)-7-((S)-2-methyl-3-pyrrolidin-1-ylpropoxy)-1-oxo-1H-isoquinolin-2-yl]-N-isopropylacetamide; antidepressants; hypothalamo-pituitary-adrenal axis modulators Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative of formula I, or pharmaceutically acceptable salts or solvates thereof wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives according to the present invention and their use in therapy.
WO2008031888A2 Condensed pyrimidinones active on glutamatergic receptors The present invention relates to a compound of Formula (I) process for its preparation and uses thereof.
WO2011091719A1 Crystalline hydrates of alkyl acyl acetaldehyde sulfite, preparation methods and uses thereof Crystalline hydrates of alkyl acyl acetaldehyde sulfites, preparation methods and uses thereof. The molecular formula of the hydrates of alkyl acyl acetaldehyde sulfites is CnH2n+1C(O)CH2CH(OH)SO3M·mH2O, wherein n=8-14, m=0.2-1.5, M is NH4 +, Na+, K+, a pharmaceutically acceptable metal ion or an organic base. Compared with anhydrides of alkyl acyl acetaldehyde sulfites, the hydrates of alkyl acyl acetaldehyde sulfites have low hygroscopicity, therefore can be stored stably, and are convenient to transport and be formulated into preparations.
US20120149748 Pharmaceutical Cream Compositions and Methods of Use The present invention provides pharmaceutical cream compositions comprising oxymetazoline and methods for treating rosacea and other skin disorders as described herein using the above cream compositions.
US20110301207 Methods and sustained release nicotinic acid compositions for treating hyperlipidemia An orally administered antihyperlipidemia composition according to the present invention includes from about 250 to about 3000 parts by weight of nicotinic acid, and from about 5 to about 50 parts by weight of hydroxypropyl methylcellulose. Also, a method of treating hyperlipidemia in a hyperlipidemic having a substantially periodic physiological loss of consciousness, includes the steps of forming a composition having an effective antihyperlipidemic amount of nicotinic acid and a time release sustaining amount of a swelling agent. The method also includes the step of orally administering the composition to the hyperlipidemic once per day “nocturnally,” that is in the evening or at night.
CN102370642A Amoxicillin medicinal composition and preparation method thereof The invention discloses an amoxicillin medicinal composition and a preparation method thereof, which are used for increasing the dissolution rate of amoxicillin in water and enhance the in-vivo absorption of amoxicillin. According to the specific technical scheme, the amoxicillin medicinal composition comprises amoxicillin, polyethylene glycol and hydroxymethyl propyl cellulose, wherein the polyethylene glycol is preferably polyethylene glycol 6000; and the weight ratio of the amoxicillin to the polyethylene glycol is 5:1-1:1. The method for preparing the amoxicillin medicinal composition comprises the following steps of: (1) dissolving; (2) drying; (3) screening; and (4) tableting. According to the invention, the problems of low solubility and unstable absorption of amoxicillin are solved, and the medicament effect is enhanced. The amoxicillin medicinal composition is suitable for treating infection caused by sensitive bacteria, upper respiratory tract infection such as otitis media, nasosinusitis, tonsillitis and the like, uropoiesis and reproduction infection, skin soft tissue infection and lower respiratory tract infection.
WO2008041090A1 Malanin concentrating hormone receptor-1 antagonist pyridinones The present invention provides for MCHR1 antagonist compounds of formula (I), and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein the substituents are as defined herein, and the pharmaceutically acceptable salts, solvates and prodrugs thereof, which are useful in treating diseases or conditions wherein antagonism of the MCHR1 receptor is beneficial.
US7109179 Methods and compositions comprising DNA damaging agents and p53 The present invention relates to the use of tumor suppressor genes in combination with a DNA damaging agent or factor for use in killing cells, and in particular cancerous cells. A tumor suppressor gene, p53, was delivered via a recombinant adenovirus-mediated gene transfer both in vitro and in vivo, in combination with a chemotherapeutic agent. Treated cells underwent apoptosis with specific DNA fragmentation. Direct injection of the p53-adenovirus construct into tumors subcutaneously, followed by intraperitoneal administration of a DNA damaging agent, cisplatin, induced massive apoptotic destruction of the tumors. The invention also provides for the clinical application of a regimen combining gene replacement using replication-deficient wild-type p53 adenovirus and DNA-damaging drugs for treatment of human cancer.
CN103664993A Compounds for treating ischemic brain injury and application thereof The invention discloses compounds, and a pharmaceutical composition and new application thereof in preparing medicines for treating ischemic brain injury. The compounds for treating ischemic brain injury can have very obvious effect.
US20080242734 Amantadine therapeutic for treatment and prevention of enterovirus (EV) or encephalomyocarditis virus (EMCV) infection The present invention relates to use of bicistronic DNA constructs for identifying compounds that inhibits IRES-dependent translation activity of an infectious enterovirus (EV) or encephalomyocarditis virus (EMCV) without affecting CAP-dependent translation activity of a host subject. The compounds thus identified are useful in preparation of a medicament for treating EV or EMCV infection.
US7476657 Appear to function at least in part by inhibiting G2 cell cycle checkpoint; useful in treating metastatic and non-metastatic solid or liquid tumors This invention provides compounds including peptides and peptidomimetics that can be used to treat cell proliferative disorders, such as those associated with benign and malignant tumor cells. While the invention is not limited to any particular mechanism, the compounds of the invention appear to function at least in part by inhibiting G2 cell cycle checkpoint. Thus, invention compounds can be used to inhibit cell growth alone or be used in combination with a nucleic acid damaging treatment to inhibit cell growth.
US20090082329 Novel Sulphur-Containing Cyclic Urea Derivatives, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors The disclosure relates to compounds of formula (I): wherein Ra, Rb, R, and n are as defined in the disclosure, to pharmaceutical compositions comprising said compounds, and to processes for making and methods of using the same.
US20050014731 Treatment of Th1 dominated immunological disease states with non-endogenous gestagen compounds A method of treating and/or inhibiting immunological disease states which are associated with a Th1 dominated reaction pattern of the pathological immune response by administering to a patient in need thereof an effective amount of at least one non-endogenous gestagen compound.
CN101352408A Alficetin in situ forming eye gel The invention discloses a chloramphenicol eye ophthalmic gel and a preparation method thereof; every 1000ml of the chloramphenicol eye ophthalmic gel contains 5-50g of chloramphenicol, 0.05-1g of preservative, 1.0-7.5g of osmoregulation agent, 30-150g of gel stroma, and rest amount of acid-base buffering agent and water used for injection. Due to the optimization and technique improvement of the auxiliary materials, the medicine dosage forms of the chloramphenicol are enriched, detention time of the medicine in the eyes are greatly prolonged, and the medicine can exert the drug effect, thus not only improving healing efficacy, but also reducing the times and days for taking medicine, decreasing the part side effect of the medicine and the untoward effect caused by the whole body absorption, as well as having no pessimal stimulation response.
CA2190943C Pharmaceutical compositions comprising an opiate antagonist and calcium salts, their use for the treatment of endorphin-mediated pathologies The combined use of opiate antagonists and of calcium salts for the preparation of medicaments for the treatment of endorphin-mediated pathologies is described.
DE102006006893B3 New aspoquinolone compounds useful in the preparation of anti-proliferative therapeutics Aspoquinolone compounds (Ia-Id) are new. Aspoquinolone compounds of formula (Ia-Id) are new. An INDEPENDENT CLAIM is included for the preparation of (I). [Image] [Image]
CN102114029A Water-soluble vitamin powder injection without preservative and preparation method thereof The invention provides a water-soluble vitamin powder injection and a preparation method thereof, in particular a water-soluble vitamin powder injection without a preservative and a preparation method thereof. The product provided by the invention is a water-soluble vitamin powder injection without a methylparaben preservative, has favorable biological stability equivalent to or superior to similar products containing the methylparaben preservative on markets, and also has better safety and clinical survivability.
US20110251253 Solid forms of (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
WO2007060249A1 Aminophenylsulfonamide derivatives as hiv protease inhibitor The present invention concerns substituted aminophenylsulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present substituted aminophenylsulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
EP2606887A1 Diindolylmethane, precursor and derivatives thereof in preparation of medicaments for treating liver diseases This invention relates to biopharmaceutical technology, specifically to the application of 3,3'-Diindolylmethane, indole-3-carbinol, and derivatives thereof in the preparation of drugs for treating such hepatic diseases as viral hepatitis, alcoholic hepatitis, drug-induced hepatitis, fatty liver, hepatic fibrosis and hepatic cirrhosis. The said indole-3-carbinol, diindolylmethane and derivatives thereof can effectively protect the human body from the damage resulting from ROS by inhibiting ROS-induced activation of hepatic stellate cells and correlated expression of collagen, which consequently ameliorates degree of hepatic fibrosis. Therefore they can be used in treatment of diseases related to hepatic fibrosis. As is verified in the animal models of hepatic fibrosis, the said indole-3-carbinol, diindolylmethane and derivatives thereof present excellent therapeutic effect and positive application prospect.
US20050072272 Combustion of mixed gas of oxygen and hydrogen in high pressure water; melting titanium in combustion gas; health, cosmetics and medical equipment utilize physiologically activating effect; water electrolysis apparatus for generating the mixed gas This invention provides a method and apparatus for manufacturing titanium-dissolved water with molten titanium dissolved therein, the molten titanium being titanium metal melted by the combustion gas resulting from the combustion of a mixed gas of oxygen and hydrogen in high-pressure water, as well as the resultant titanium-dissolved water and health articles, medical articles and cosmetics utilizing the physiologically activating effect of the high-function water containing titanium.
US20060189535 Combination treatment using exendins and thiazolidinediones The present invention relates to methods for treatment and/or prevention of diabetes and diabetes related diseases. More specifically, the methods and uses of the invention pertains to administration of an exendin-4 compound in combination with administration of a thiazolidinedione insulin sensitizer.
US7271146 Methods for treatment of Helicobacter pylori-associated disorders The present invention relates to methods for treating pathological conditions associated with Helicobacter sp infections, specifically H. pylori infection. The present invention further relates to methods for treating pathologies characterized by excess gastric acid secretion. The methods of the present invention comprise oral administration of pentagastrin effective locally in the stomach in conjunction with a gastric proton pump inhibitor. It is disclosed herein for the first time that PG administered orally exerts a local effect in the stomach and may be used in combination with a PPI for treating pathological conditions characterized by excess gastric acid secretion and in pathological conditions associated with Helicobacter sp infections.
DE102004049622A1 Novel para-sulfonamido-substituted 2-anilinopyrimidines are useful in a wide range of medicaments and as cell cycle kinase inhibitors or receptor tyrosine kinase inhibitors Para-sulfonamido-substituted 2-anilinopyrimidines and their isomers, diastereomers, enantiomers and/or salts are new. Para-sulfonamido-substituted 2-anilinopyrimidines of formula (I) and their isomers, diastereomers, enantiomers and/or salts are new. A and D : halogen, hydroxy, cyano, -OR5>, 3-6C cycloalkyl or 1-4C optionally branched alkyl optionally once or more substituted by halogen, hydroxy or OR5>; X : -NH-, -N(1-3C optionally branched alkyl)- or -O-; R1>halogen or cyano; R2>1-3C alkoxy-substituted hydroxy-1-8C optionally branched alkyl or hydroxy- or 1-3C alkyl-substituted 3-7C cycloalkyl; R3> and R4>H or 1-3C optionally branched alkyl optionally once or more substituted by hydroxy, -OR5> or -NR6>R7>; R5>optionally halogen-substituted 1-4C optionally branched alkyl; and R6> and R7>1-3C alkyl optionally substituted by hydroxy or -OR5>. Independent claims are also included for (1) the use in the preparation of (I) of acetylaminobenzene sulfonyl halides or acetylaminobenzene sulfonamides of formula (IIa) and (IIb) respectively or their isomers, diastereomers, enantiomers and/or salts; and (2) pharmaceuticals including (I). [Image] - ACTIVITY : Cytostatic; Ophthalmological; Immunosuppressive; Dermatological; Antiinflammatory; Cardiant; Nephrotropic; Virucide; Vulnery; Hepatropic; Antiarteriosclerotic; Vasotropic; Antidiabetic; Antipsoriatic; Thrombolytic; Antiparkinsonian; Nootropic; Neuroprotective; Anti-HIV; Anticonvulsant; Antirheumatic. - MECHANISM OF ACTION : (I) can inhibit proliferation of tumor cells and/or tumor angiogenesis with simultaneous reduction of side effects by a carboanhydrase effect. Proliferation tests of 4-[5-Bromo-4-((R)-2-hydroxy-1-dimethyl ethylamino)-pyrimidin-2-ylamino]-2,6-dimethylbenzenesulfonamide with mamma carcinoma cells (MCF7), prostate carcinoma cells (DU145) and multiply-resistant mamma carcinoma cells (MaTu-MDR) gave proliferation values (IC50) of below 0.1, 0.09 and 0.07 mu M respectively, the corresponding values for a control comprising the pyrimidine compound of Example 10 of being 0.4, 0.7 and 0.8 mu M.
EP2742940A1 Salts of aza-bicyclo-di-aryl ethers for adminstration once daily, twice daily or thrice daily The invention relates to an administration unit comprising a fumarate, maleate, chloride, phosphate, succinate or malonate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane for use in the treatment of a disorder or a disease in a human, wherein the administration unit is administered once daily, twice daily or thrice daily, and to a packaging comprising the administration unit according to the invention.
US20050095686 Preparing starch composition to improve structure, texture and stability of food; for use in prevention and treatment of infection, immunological and tumor disorders A method for producing a beta-glucan from a non-pathogenic saprophytic filamentous fuingus or composition that contains it. Also, methods for providing this beta-glucan in a food product to improve structure, texture, stability or combinations thereof, in a food product to provide nutrition or in the manufacture of a medicament or nutritional composition for the prevention or treatment of an immune disorder, tumor or microbial infection.
CN102008465A Application of macrolide compound from marine microorganisms in preparing anti-tumor medicines The invention relates to the technical field of medicines. Due to the particularity of the marine environment and the diversity of marine microorganisms, the search of new anti-tumor activity lead compounds in active metabolic products of the marine microorganisms becomes the current study hotspot. The invention provides application of a macrolide compound Macrolactin Q from the marine microorganism in preparing anti-tumor medicines. The Macrolactin Q has high cytotoxicity on various human tumor cell strains and animal tumor strains in the microgram concentration level, and has high anti-tumor effect on nude mouse models of the animal tumor strains. The invention provides lead compounds for studying and developing novel anti-tumor medicines and the lead compound is a potential anti-tumor medicine.
CN1739541A Puerarin prepn for eye and its prepn process The puerarin preparation for eye is prepared with puerarin as active component and supplementary material. The present invention also provides the preparation process of the puerarin preparation for eye. The puerarin preparation for eye is one kind of eye drop with low viscosity, and after being dropped into eye, it will take phase conversion in the physiological condition inside eye to change into gel prolonging the retention period for high bioavailability.
US20110173709 Ectopic, orthotopic model for revascularization and tumor assessment Improved vascularization and tumor models, comprising a test animal having a dorsal skin window chamber, and an exogenous tissue sample implanted ectopically in the skin within the window chamber, are described, as are methods of using the models.
US8178574 Tosylate salt of trans-N-isobutyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-yl-methyl)-phenyl] cyclobut anecarboxamide The present invention is directed to the tosylate salt of trans-N-isobutyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide Formula (I): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.
CA2664145A1 Use of a mt kinase inhibitor for treating or preventing brain cancer The present invention is concerned with the finding that some the macrocyclic quinazoline derivative 4,6-ethanediylidenepyrimido[4,5-b][6,1,12]benzoxadiazacyclo-pentadecine, 17-bromo-8,9,10,11,12,13,14,19-octahydro-20-methoxy-13-methyl-, described as compound 22 in PCT publication WO2004/105765, is useful in the manufacture of a medicament for the treatment or prevention of a primary brain cancer or brain metastasis. It accordingly provides methods for treating, preventing, delaying or mitigating brain cancer, or for preventing or slowing proliferation of cells of brain origin.
WO2005053675A1 A composition comprising the alcohol compound isolated from the extract of cucurbitaceae family plant having anti-adipogenic and anti-obesity activity The present invention is related to an alcohol compound isolated from the extract of Cucurbitaceae family plant having anti-adipogenic and anti-obesity activity, and a composition comprising the same. The compound showed potent reducing activity of body weight, decreasing effect on the blood triglyceride and cholesterol level, activating activity of PPAR alpha and preventing activity from the adipogenesis of precursor fat cells with no toxicity, therefore, those compound can be useful in treating or preventing obesity and adipogenesis-involved diseases as a medicine or health care food.
WO2006099352A1 Novel isophthalates as beta-secretase inhibitors There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
CN102327219A Solid esomeprazole magnesium lipidosome preparation The invention relates to a solid esomeprazole magnesium lipidosome preparation and a preparation method thereof. The solid esomeprazole magnesium lipidosome preparation is characterized by mainly comprising the following components according to weight part: 20 parts of esomeprazole magnesium, 50-100 parts of soybean lecithin, 50-150 parts of distearoyl phosphatidylglycerole, 50-150 parts of cholesterol and 150-200 parts of other general pharmaceutical excipients. According to the invention, the solid esomeprazole magnesium lipidosome preparation is prepared by adopting a reverse phase evaporation method, thus the bioavailability and the stability of the esomeprazole magnesium are greatly improved, toxic or side effects are greatly reduced, the quality of a preparation product and the curative effect is improved and the convenience for the clinical application is greatly realized.
WO2010142167A1 New use of carboxyamidotriazole compounds or salts thereof in the preparation of the medicaments for preventing and treating interstitial pneumonia or pulmonary fibrosis The present invention provides the use of carboxyamidotriazole or pharmaceutically acceptable salts, analogues or derivatives thereof in the preparation of the medicaments for preventing or treating interstitial pneumonia or pulmonary fibrosis. The interstitial pneumonia or pulmonary fibrosis includes lithicosis, sarcoid, allergic pneumonia, drug-induced pneumonia, radiation pneumonia, infection, fibrosing alveolitis related to collagen vascular diseases. The present invention also provides the drug kits comprising the carboxyamidotriazole compounds.
US20070066536 Methods for treating hormone associated conditions using a combination of LHRH antagonists and specific estrogen receptor modulators Methods for treating hormone associated conditions, such as endometriosis, uterine leiomata, ovarian cancer, breast cancer, or vaginal bleeding, using LHRH antagonists and selective estrogen receptor modulators are disclosed. The methods include administering to a subject a combination of an LHRH antagonist and a selective estrogen receptor modulator. Pharmaceutical compositions and kits for use in the methods of the invention are also provided.
US20120208767 Method to Detect or Treat Painful Bladder Syndrome based on Relation to Quinone Oxidoreductase 1 A method includes obtaining a biological sample from a subject that does not display a symptom of Painful Bladder Syndrome (PBS). The method also includes analyzing the biological sample for a mutated form of NAD(P)H dehydrogenase [quinone], also known as Quinone Oxidoreductase 1, abbreviated NQO1, or a mutation of a NQO1 gene. The method also includes determining a risk of PBS for the subject based on analyzing the biological sample. In some methods, the mutation determined to present an increased risk is a cytosine to thymine nucleotide substitution at a position that leads to a proline to serine amino acid substitution at amino acid position 187 to produce a protein NQO1P187S. Another method includes selecting a subject that has above normal risk of Painful Bladder Syndrome (PBS) or is expressing a symptom of PBS, and treating the subject with a therapeutically effective amount of an antioxidant.
CN102579447A Preparation method for anti-tuberculosis medicinal compound preparation The invention belongs to the technical field of medicine, and relates to a preparation method of an anti-tuberculosis edicinal compound preparation containing rifampicin, retozide, pyrazinamide and ethambutol hydrochloride. The method comprises the following steps of: granulating rifampicin by adopting a dry pelletizing technology; granulating two or three of the retozide, pyrazinamide and ethambutol hydrochloride by adopting a wet preparation technology or a dry preparation technology; and pressing into dual-layer tablets or multi-layer tablets of rifampicin, retozide, pyrazinamide and ethambutol hydrochloride. The preparation method aims to avoid generation or acceleration of degradation caused by close contact of rifampicin with other medicaments in a preparation, so that the stability of a compound rifampicin preparation is ensured.
WO2006115871A1 Extended estrogen dosing contraceptive regimen A method of contraception that provides for sequentially administering to a female of child bearing age: (a) a first composition containing a progestin in an amount equivalent to about 0.3 to about 1.5 mg norethindrone acetate and an estrogen in an amount equivalent to about 5 to about 20 meg of ethinyl estradiol for about 22 to about 26 days; (b) a second composition containing an estrogen in an amount equivalent to about 5 to about 20 meg of ethinyl estradiol for about 2 to about 3 days and an optional third composition that is a placebo provided that (i) if estrogen administration is continuous then the first composition is administered for 25 to 26 days, the second composition is administered for 2 to 3 days and no third composition is administered and (ii) if estrogen administration is not continuous then the first composition is administered for 22 to 24 days, the second composition is administered for 2 to 3 days and the third composition is administered for 1 to 4 days. The total cycle length is 28 days, with the first composition administered on day 1 of the menstrual cycle, defined as the first day of menstrual bleeding, or on the first Sunday after the first day of the menstrual cycle.
CN103585133A Method for preparing cancer cell targeted cell-like micro-capsules The invention discloses a method for preparing cancer cell targeted cell-like micro-capsules. Endothelial cells of human umbilical veins are used as raw materials for preparing cell-like micro-capsules with amino groups on surfaces, and the micro-capsules are dispersed in an aptamer solution containing aldehyde groups; after a certain period of incubation, aptamers are marked on the surfaces of the cell-like micro-capsules and then washed with a phosphate buffer solution; and the processed cell-like micro-capsules are immersed into a drug solution of doxorubicin hydrochloride, drugs are loaded through electrostatic interaction, and finally, the cell-like micro-capsules different in drug loading capacity are obtained. The preparation method is simple, controllable, wide in material source, high in production efficiency, capable of adjusting the drug loading capacity of the cell-like micro-capsules conveniently and providing the characteristics of target cancer cells simultaneously and good in application prospect.
CN101708185A Application of cinnabar and other mercurides in preparing anti-therioma medicaments and application of mercurides in preparing antibacterial medicaments The invention discloses application of cinnabar and other mercurides in preparing anti-therioma medicaments, and simultaneously discloses application of the mercurides in preparing antibacterial medicaments. The problems of long treatment process, easily metastasizing therioma, high death rate and the like exist in the processes of treating therioma. The invention is invented for solving the problems. Because the mercurides have the characteristics of inactivating all proteins, the mercurides are lethally destructive to the DNA of various malignancies and the DNA in various bacteria, thereby achieving the aim of resisting various therioma and various bacteria.
WO2014091078A1 Polymeric particles-based temozolomide dosage form The invention relates to pharmacology and medicine, and more specifically to slow-release antitumor drug composition based on biodegradable poly(lactic-co-glycolic acid) (PLGA). The composition comprises temozolomide (TMZ) as the active ingredient and comprises, in addition, surface-active material and a cryoprotectant as parts of nanoparticles.
CN102382098A Bruguiera gymnorrhiza 5 (BG5) as well as preparation method and application thereof The invention relates to the technical field of medicines, in particular to a novel dinaphthaline spiro bruguiera gymnorrhiza 5 (BG5) compound separated from bruguiera gymnorrhiza in China, a preparation method of the dinaphthaline spiro bruguiera gymnorrhiza 5 (BG5) compound and application of the novel dinaphthaline spiro bruguiera gymnorrhiza 5 (BG5) compound to tumor treatment. The bruguiera gymnorrhiza 5 (BG5) disclosed by the invention has a structural formula shown in the description. Verified by tests, the compound has remarkable inhibitory activities for HL60 human leukemia cells and MCF (Macrophage Chemotatic Factor)-7 human breast cancer cells.
US20090012118 Kynurenic Acid Amide Derivatives as Nr2b Receptor Antagoni The new kynurenic acid amide derivatives of formula (I): and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.
CA2347913C Oral administration of adenosine analogs Disclosed are compositions including an adenosine analog, wherein the composition comprises a dosage form suitable for oral (co)administration. Also disclosed are compositions including adenosine analogs, wherein the composition is in a dosage form including a pill, capsule, lozenge, or tablet, and compositions including adenosine analogs, wherein the composition is in a dosage form comprising a liquid. Additionally disclosed are methods of administering the inventive composition, and kits including the inventive compositions.
US6908917 Chromone derivatives as matrix metalloproteinase inhibitors This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, Y2, Y3, Y4, U5, U6, U8, and R2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.
EP2552893A1 Antibacterial isoquinolin-3-ylurea derivatives The invention relates to isoquinolin-3-ylurea derivatives of formula (I) wherein R1 represents (C1-C3)alkyl, (C1-C3)haloalkyl or cyclopropyl, R4 represents H and the substituents R2 and R3 and R5 have the meanings disclosed in the specification; and to the salts of such compounds. These compounds are useful for the prevention or the treatment of bacterial infections.
US20080241157 Nerve cell growth modulators (amphibodies) The present invention relates to a nerve cell growth modulator denoted an amphibody. The amphibody according to the invention is comprised of at least two components, wherein a first component is capable of binding to a target and suppressing, or essentially neutralising, a nerve cell growth inhibitory effect thereof; and a second component is capable of stimulating nerve cell growth and/or regeneration. In the most preferred embodiment, the present amphibody is a neuromodulator comprised of the above disclosed two components connected by a linker element. Amphibodies according to the invention are a useful means of molecular disguise of a non-permissive environment into a permissive, and outgrowth promotive and favorable one. The present invention also relates to genetic and chemical methods of preparation of an amphibody according to the invention as well as to various advantageous uses thereof.
WO2013107189A1 Gambogenic acid derivatives, preparation method and application thereof Disclosed are gambogenic acid derivatives having a structure shown as formula (I) or (II), salts, preparation method and application thereof in the treatment of tumor. Compared with gambogenic acid, the gambogenic acid derivatives exhibit more potent anti-tumor activities.
CN102824354A Application of polydatin in preparation of pharmaceuticals for preventing and treating chronic glomerular diseases The invention relates to a new pharmaceutical application of natural monomeric compound polydatin and specifically relates to an application of polydatin in preparation of pharmaceuticals for preventing and treating chronic glomerular diseases, particularly for preventing and treating progressive chronic glomerular diseases and sertoli cell cytopathic (such as glomerulosclerosis and the like) glomerular diseases. Animal experimental results show that the polydatin has obvious functions of preventing and improving the glomerulus functions and organic cause damages of a fructose model rat, and also has obvious functions of preventing and improving the urine protein and glomerulus sertoli cell damage of a glomerulosclerosis model rat. The polydatin and related adjuvants are mixed to be prepared into healthcare products or pharmaceuticals for preventing and treating glomerular diseases by a conventional preparation method; and the polydatin can be applicable to glomerulosclerosis and other diseases which relate to sertoli cell cytopathy and is capable of delaying and improving the glomerular progressive disease courses of related diseases.
WO2007034282A3 Diaryl-imidazole compounds condensed with a heterocycle as c3a receptor antagonists Aryl substituted imidazo[4,5-c] pyridine compounds are provided. These compounds are useful in pharmaceutical compositions as C3a antagonists for treating a variety of medical conditions associated with the Complement cascade. Methods for treating such conditions are also provided.
US20110105547 Filamin a-binding anti-inflammatory analgesic A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within.
WO2013031620A1 Osteogenesis promoter and use thereof The purpose of the present invention is to provide an osteogenesis promoter that can be administered locally and systemically and that is suitable for clinical application. Provided is an osteogenesis promoter that contains, as an active ingredient, at least one compound selected from the group consisting of phenazopyridine hydrochloride, riluzole hydrochloride, tranilast, rabeprazole, indoprofen, nabumetone, luteolin, leflunomide, lansoprazole, methiazole, thiabendazole, albendazole, tiaprofenic acid, balsalazide sodium salt, and cyclosporin A, or a pharmaceutically acceptable salt thereof. Preferably, rabeprazole or lansoprazole, which are proton pump inhibitors, is used as an active ingredient.
CN102670491A Sodium ozagrel sodium chloride injection and preparation method thereof The invention provides a sodium ozagrel sodium chloride injection and a preparation method thereof and belongs to the technical field of medicines. The invention aims to overcome the defects that a traditional sodium ozagrel raw material is high in cost and cannot meet the market demand, and moreover, the preparation technology is complicated due to the fact that sodium ozagrel and the sodium ozagrel sodium chloride injection are separately prepared. The injection comprises the following components in parts by weight: 70-75 parts of ozagrel, 140-150 parts of glycine, 5-15 parts of citric acid, 25-35 parts of sodium hydroxide and 850-900 parts of sodium chloride. The invention also provides the preparation method for the sodium ozagrel sodium chloride injection. The sodium ozagrel sodium chloride injection provided by the invention is high in stability and is obtained by directly synthetizing the sodium ozagrel during the preparation process. The raw material is low in cost, the technical process is simple, and the cost is low.
US7220735 And aza- and diaza-derivatives thereof; especially treating allergy or nasal congestion Disclosed are novel compounds of the formula wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally substituted aryl or heteroaryl, and the remaining variables are as defined in the specification, and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.
CA2817982A1 Controlled release mucoadhesive systems Formulations for chemoprevention of oral cancer and precancerous lesions, and for methods for preparing the formulations are described.
US20120022083 Small molecule modulators of cell adhesion Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.
WO2007064945A3 Cancer therapies and pharmaceutical compositions used therein The invention relates to compositions and methods to inhibit gene expression. In particular, the invention provides co-therapies comprising oligonucleotides plus other therapies to treat cancer.
EP1832580A1 Crystal and salt of 1-cyclopropylmethyl-4-ý2-(3,3,5,5)-tetramethylcyclohexyl)phenyl¨piperazine Salts and crystals of 1-cyclopropylmethyl-4-[2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine have excellent cell adhesion inhibitory action and cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis.
CN103342726A Preparation method and application of camellia flavonoid for reducing blood glucose The invention relates to a preparation method and application of camellia flavonoid for reducing blood glucose. The camellia flavonoid is kaempferol-3-0-[2-O-beta-D- xylose-6-O-alpha-rhamnose]-beta-D-glucoside. Compared with the prior art, the preparation method of the camellia flavonoid for reducing the blood glucose has the following beneficial effects that seed cakes obtained after the camellia seed is squeezed for oil extraction are applied to the preparation and separation of the active ingredient for reducing the blood glucose; and the camellia flavonoid obtained by using the preparation method provided by the invention can be used as a medicine and healthcare food for diabetes mellitus, has good blood glucose reducing effect and hardly damages a human body.
WO2012103226A3 Bendamustine formulations Aspects of the present appliction relate to pharmaceutical formulations comprising bendamustine or its pharmaceutically acceptable salts, isomers, racemates, enantiomers, hydrates, solvates, metabolites, polymorphs, and mixtures therof, suitable for phamaceutical use. Aspects further provide methods of producing stable bendamustine compositions.
US20120190664 Process for the preparation of antibiotic compounds The present invention relates to a process for the preparation of carbapenem antibiotic compounds, which are useful for intravenous and intramuscular administration.
CN101837011A Medicinal composition for treating diabetes The invention discloses a medicinal composition for treating diabetes, which has a function like that of insulin, and comprises a chromium salt and an adenosine phosphate, which are medicinal active ingredients accounting for 1 to 95 weight percent of the composition; the chromium salt is trivalent chromium salt which is pharmaceutically soluble; and the adenosine phosphate may be adenosine phosphate (AMP), adenosine diphosphate (ADP) or adenosine triphosphate (ATP), or may be a derivative of the AMP, a derivative of the ADP and a derivative of ATP, or may be 3',5'-cyclic adenosine monophosphate. The medicinal composition may also contain cysteine. The medicinal composition has a function like that of insulin, can directly promote the absorption of amylaceum, contributes to blood sugar control, promotes the normal glycometabolism of body and the normal lipid metabolism of the body and can be used for treating diabetes and diseases associated with the diabetes.
CN1561973A External long-acting analgesic An externally-applied durable analgetic is proportionally prepared from menthol, alcohol solution, the water for injection, lidocaine hydrochloride, glycerine and polysorbate.
EP1572665A2 1-n-phenylamino-1h-imidazole derivatives as aromatase inhibitors The present invention relates to imidazole derivatives of the formula: (I) in which R1, R2, R3, R4, R5, R6 and n are as defined in the specification.The invention also relates to pharmaceutical compositions containing these derivatives, and to the uses thereof.
US20080182841 Sustained release bioadhesive carrier such as polycarbophil; coronary antiarrhythmic; local anesthetic; calcium channel blocker; autocoid; antiprostaglandin; nonsteroidal antiinflammatory; cyclooxygenase, thromboxane or leukotriene inhibitor; infertility The invention relates to a pharmaceutical composition for relieving pelvic pain or infertility associated with uterine dysrhythmia. The composition includes a locally-administered anti-dysrhythmic treating agent and a bioadhesive extended-release carrier. The composition may be delivered in an extended release formulation that includes a bioadhesive, water-swellable, water-insoluble, cross-linked polycarboxylic acid polymer, such as polycarbophil. The treating agent may be a local anesthetic, such as lidocaine. The invention also relates to a method of treating or preventing pelvic pain, or treating or improving infertility, by inserting a mixture of an anti-dysrhythmic treating agent and a bioadhesive carrier into the vagina of the patient to be treated.
WO2009016085A1 Spiro compounds useful as antagonists of the h1 receptor The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.
CA2362343C Method and composition for treating acne The present invention provides a method for treating acne vulgaris by serially applying a topical composition of azelaic acid and a topical composition of benzoyl peroxide. The present invention also provides topical compositions of a peroxide of benzoyl peroxide, and azelaic acid and its derivatives, such as azelaic acid, sodium salt or methylester which are useful for treating acne vulgaris and may be used to simultaneously apply benzoyl peroxide and azelaic acid.
US20060093656 Warming patch A warming patch 10 comprising a support 2 and adhesive layer 1 disposed on at least one surface of this support 2, wherein the adhesive, layer 1 contains a warming material, 1-menthol and polyethylene glycol as an irritation reducing agent.
CN1969910A Drop pills containing panax notoginsenosides for treating cardiovascular and cerebrovascular disease and preparation process thereof The invention relates to a medicament for treating cardiovascular and cerebrovascular diseases and after-effects, in particular a kind of dripping pills and the process for preparation, wherein the active constituents comprise (by weight portions) panax notoginseng saponins and borneo camphor by a weight ratio of 15-50:1.
CN103012618A Preparation method of switch type NO procedural donor The invention relates to a preparation method of a switch type NO procedural donor. The preparation method comprises the following steps in sequence: adding chitosan or chitosan derivatives which are grafted with molecular switch functional groups to absolute methanol solution of sodium methoxide; introducing NO; reacting in a pressurizing condition so as to obtain a NO donor; substituting by O2, thus obtaining the O2-substitued NO donor; and then obtaining a nucleophilic NO donor with the stimuli responsive type molecular switch function and an O2-substitued derivate of the nucleophilic NO donor by utilizing the photo-isomerization or temperature-isomerizationfunction of the switch type functional group, wherein the nucleophilic NO donor can realize a procedural control release process of opening the door to release NO once NO is generated in a target organ or a target cell under the molecular level. Compared with the prior art, the preparation method provided by the invention is simple and convenient; and the prepared compound is applicable to releasing the NO and other medicines under procedural control.
US20100172896 Hmgb1 protein inhibitors and/or antagonists for the treatment of vascular diseases A method of inhibiting atherosclerosis by administering a molecule that binds a protein of the HMG box family. Also, a method of treating vascular diseases by administering an antagonist molecule to inhibit the interaction between a protein of the HMG box family and a receptor for the protein of the HMG box family.
WO2009106574A3 Combination comprising a cannabinoid receptor binding compound and an opioid The present invention relates to novel combinations suitable for the treatment or amelioration of pain of various genesis or aetiology, which comprise, as active ingredients, at least one cannabinoid receptor binding compound, in particular a cannabinoid receptor binding naphthalene derivative, and at least one opioid, to their preparation, to their use as medicaments and to medicaments comprising them.
US20060147401 Skin material for external use and antiprutiric agent for external use and wrinkle-instrument using the same A skin composition for external use containing an acidic composition (A) which contains an alginate(s), at least one of weak acid selected from among phosphoric acid-type weak acids and ethylenediaminetetraacetic acid-type weak acids, and water; and a solidifying/gelling agent (B) containing a calcium salt(s) which is to be supplied to the acidic composition (A) sticking to the skin surface. In some cases, the skin composition for external use further includes an absorbent to be impregnated with the acidic composition (A).
CN101601660A Soluble tablet containing clopidogrel The invention discloses a clopidogrel soluble tablet and a preparation method thereof. The soluble tablet contains an active ingredient of clopidogrel or pharmaceutically acceptable salts and pharmaceutical excipients, wherein the pharmaceutical excipients comprise soluble excipients. The ratio of the clopidogrel to the soluble excipients is 1:1-10 in percentage by weight. The soluble tablet can also contain a disintegrant and a lubricant. The preparation method for the clopidogrel soluble tablet can be a direct tabletting method or a wet granulation tabletting method. Compared with a common tablet, the clopidogrel soluble tablet has the advantages of fast disintegration and formation of solution state in water within a short period of time, is easy in storage and use and particularly convenient for a patient with swallowing difficulty, and significantly improves the compliance of the patient.
CN1875962A Prescription of silibinin-n-methylglucamine drop pills and preparation process thereof The invention relates to a medicament for treating acute and chronic hepatitis and process for preparation, wherein the medicament is prepared from silibinin-N-methylglucamine as the main constituent, and right mxtrix through a predetermined processing combinations. Compared with the existing dosage forms, the drop pill preparation has the advantages of short technological process, low cost of production and quick-effectiveness.
EP2318371A2 Novel solid state forms of laquinimod and its sodium salt Provided herein is a novel crystalline form of laquinimod, process for the preparation, pharmaceutical compositions, and method of treating thereof. Provided also herein are novel amorphous and polymorphic forms of laquinimod sodium, process for the preparation, pharmaceutical compositions, and method of treating thereof.
US20080306043 Sabcomeline Alone or Combined with a Mood Stabilising or Antimanic Agent to Treat Bipolar Disorders The invention relates to the use of sabcomeline or a pharmaceutically acceptable salt thereof in monotherapy for the treatment of bipolar disorder or mania or and to adjunctive and simultaneous combination therapies for the treatment of bipolar disorder or mania in which sabcomeline or a pharmaceutically acceptable salt thereof and at least one other mood stabilizing or antimanic agent are administered adjunctively or simultaneously. The invention provides methods of treatment of bipolar disorder or mania utilizing such monotherapy and such adjunctive or simultaneous therapeutic combination therapies, therapeutic combinations for use therein and pharmaceutical compositions comprising them.
CN103040788A Cefuroxime axetil capsule and preparation method thereof The invention discloses a cefuroxime axetil capsule. The cefuroxime axetil capsule is prepared by filling the uniformly mixed cefuroxime axetil-containing medicine-carrying pills and talcum powder into a capsule shell; and the medicine-carrying pills are prepared according to the following steps of: weighing the cefuroxime axetil and a disintegrating agent to be dissolved or dispersed in acetone, spraying the formed solution or injectable suspension to lactose pills in a fluidized bed, and coating and drying to obtain the medicine-carrying pills. The cefuroxime axetil raw material is coated on the outer layers of the lactose pills and is uniformly distributed on the surfaces of the pills, the specific surface area of the medicine is greatly increased, the raw material can be quickly released, and thus, the dissolubility and bioavailability of the medicine are improved.
US7307082 Heterocyclic derivatives as CRF antagonists This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I wherein X1 is (CH2)n or CO, n is 0 to 2 and R1, R2, R3 and R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents
CN101524546A Conjugate conjugated from polyethylene glycol and curcumin derivative The invention belongs to the field of medicinal chemistry, and more particularly relates to conjugate conjugated from polyethylene glycol and curcumin derivative as shown in formula 1 and pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently selected from nitro, amidogen, bi-low alkyl amidogen and low alkoxy; R3 and R4 are independently selected from halogen, nitro and hydrogen; R5 is low alkyl or hydrogen; R6 is hydrogen or low alkyl that can be substituted by low alkyl, nitro, hydroxide radical or sulfhydryl which are randomly selected; and n is 1 or 2. The conjugate has good water solubility, overcomes the disadvantages of poor water solubility, low bioavailability, and the like, existing in curcumin, and has low preparation cost and better antitumor activity. In addition, the invention also relates to the pharmaceutical composition, the preparation method and the application as medicament of the conjugate.
US20100092443 Novel combinations of nitrogenated heterocyclic antibacterial compounds with other antibacterial compounds and the use of same as drugs The invention relates to the combination of nitrogenated heterocyclic antibacterial compounds of formula (I) with other antibacterial compounds and the use of same as drugs. The nitrogenated heterocyclic compounds are of general formula (I) wherein R1 represents a (CH2)n-NH2 or (CH2)n—NHR radical, where R is a (C1-C6) alkyl and n is equal to 1 or 2; R2 represents a hydrogen atom; R3 and R4 together form an aromatic nitrogenated heterocycle with 5 apexes with 1, 2 or 3 nitrogen atoms optionally substituted by one or several R′ groups, R′ being selected in the group composed of a hydrogen atom and the alkyl radicals with 1 to 6 carbon atoms, in free form, as zwitterions, and in the form of salts of pharmaceutically acceptable inorganic or organic bases and acids. The other antibacterial compound is selected among the group comprised of beta-lactams, monobactams or penicillins, if needed combined with a beta lactamases inhibitor, aminoglycosides, glycylcyclines, tetracyclines, quinolones, glycopeptides, lipopeptides, macrolides, ketolides, lincosamides, streptogramins, oxazolidinones, polymyxins and other compounds known to have therapeutic activity on Pseudomonas aeruginosa and Enterobacteriaceae.
US20110003811 Subsituted pyridine derivatives The present invention relates to pyridine derivatives of the general formula (I) and their use as openers of the KCNQ family potassium ion channels for the treatment of CNS disorders.
WO2007129725A1 Agent for preventing liver disease Disclosed are an agent for preventing a liver disease, an agent for preventing an alcoholic liver disease, and the like. Specifically, disclosed is an agent for preventing a liver disease, comprising hydroxyproline or an N-acylated hydroxyproline or a salt thereof as an active ingredient.
CN103655609A Medicine for treating tinea of feet and hands The invention discloses a medicine for treating tinea of feet and hands. The medicine is characterized by being prepared by the following method: weighing 1500 parts of rice vinegar, 100 parts of alumen, 50 parts of salt and 10 parts of aspirin in part by weight, mixing with 20-23 parts of carbolic acid, heating till a boiling state, cooling to room temperature, and packaging. The medicine prepared by the method has a very significant effect on the tinea of the feet and the hands; the treatment time is short; the cure rate is high; generally, the hands are soaked by the medicine for 30-40 minutes every time, and after continuous use of 6-15 days, the tinea can be cured, with 6 days for light tinea and 15 days for serious tinea; and within 6 years, the using effects on 334 patients show that the effective rate is as high as 100%, the cure rate is as high as 95.5% and the tinea of the feet and the hands does not recur after being cured.
WO2009071957A3 Novel peptides and amino acid derivatives, pharmaceutical compositions containing same and the use of these compounds The invention relates to novel compounds of general formula (I) with neurogenic or non-neurogenic anti-inflammatory, analgetic as well as tumour inhibiting effects as well as the salts and metal complexes of these compounds. In the above formula the most important meanings of the substituents are as follows: n stands for 0 or 1, and if n is 1, then Q1, Q2 and Q3 each stand for 0; R1 and R2 stand, independently from each other, for an amino acid; if n is 0, then Q1 and Q2 stand for an amino acid residue; Q3 stands for a valency bond or an amino acid residue; R1 stands for H or C1-3 acyl, benzyloxycarbonyl, tert-butyloxycarbonyl or 9-fluorenyl-methyloxycarbonyl; R2 stands for OH, -NH-R3 or -O-R4, wherein R3 stands for H, C1-6 alkyl, C6-10 cycloalkyl or C6-10 aryl; and R4 stands for C1-6 alkyl, benzyl or 9-fluorenylmethyl. Furthermore, the invention relates to a pharmaceutical composition for treating neurogenic or non-neurogenic inflammations, pains and tumour growth and to the use of the compounds of formula (I) and the salts and metal complexes thereof for preparing pharmaceuticals compositions and to a method for treating neurogenic and non-neurogenic inflammations, pains and tumour growth.
EP2136793A2 Tablet formulations containing 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one salts and tablets made therefrom Pharmaceutical formulations containing a salt of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, which are suitable for forming into a tablet dosage form, as well as tablet dosage forms are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
WO2013156772A1 Crystalline forms of (s) -4-amino-n- (1- (4 - chlorophenyl) - 3 - hydroxypropyl) -1- (7h - pyrrolo [2, 3-d] pyrimidi n-4-yl) piperidine-4-carboxamide The present invention discloses certain new solid state forms of (S)-4-amino-N-(1- (4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4- carboxamide, processes for preparing such forms, pharmaceutical compositions comprising them, and the use of such forms in therapy.
US6927209 5-thio-β-D-xylopryanoside derivatives, preparation, method, pharmaceutical compositions containing them and their therapeutic use The present invention relates to novel compounds of formula (I): in which: R1, R2 and R3, which are identical or different, are each independently: a (C1-C6)alkyl group, a pyridinyl group or a group —CH2—NR4R5, in which R4 and R5 are each independently a hydrogen atom or a (C1-C4)alkyl group, or alternatively R4 and R5 form, with the nitrogen atom to which they are bonded, a pyrrolidinyl, piperidinyl, hexahydroazepinyl, morpholinyl or piperazinyl group, with the proviso that at least one of the substituents R1, R2 and R3 is other than a (C1-C6)alkyl group, and their salts, solvates and hydrates, especially those which are pharmaceutically acceptable. These compounds are useful particularly for the treatment of disorders of the venous circulation.
US7994206 Crystals and process of making 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.
US20050106195 N-octanoyl amino acid composition for slimming the human body Use of a compound of formula (I): in which R1 represents a hydrocarbon radical comprising 7 carbon atoms, R2 represents the characterizing chain of an amino acid and m is between 1 and 50, or of a mixture of the said compounds of formula (I), as a slimming active agent. Nontherapeutic method of treatment using the said compound and use of the said compound for preparing a medicament with lipolytic activity, intended to induce slimming of the human body.
CN102038939A Preparation method of adenosine triphosphate coenzyme insulin freeze-dried powder injection The invention discloses a preparation method of an adenosine triphosphate coenzyme insulin freeze-dried powder injection, comprising the following steps of: adjusting injection water with diluted hydrochloric acid until the pH value is 2.5-3.5, adding insulin and uniformly mixing to obtain a solution I; adding L-arginine and disodium ethylene diamine tetraacetate in the injection water, uniformlystirring, adding carbon and stirring; after removing carbon, adding adenosine disodium triphosphate and uniformly stirring to obtain a solution II; adding calcium gluconate, low molecular weight dextran and cysteine hydrochloride in the injection water, adding carbon and removing the carbon and uniformly stirring to obtain a solution III; mixing three solutions, uniformly stirring, adjusting the pH value to be 5.7-6.2 with a 2-4 percent NaOH solution, adding coenzyme A and supplementing the balance of injection water; and sterilizing, measuring the content, subpackaging and freezing dry. The adenosine triphosphate coenzyme insulin freeze-dried powder injection prepared by the method has the advantages of favorable redissolution, clearness and quality stability of products and is saturatedin appearance.
US7244763 Compounds that modulate PPAR activity and methods of preparation This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.
CN102212068A Thiofuran derivative, preparation method thereof and application thereof in medicaments The invention relates to a pharmaceutical compound, a preparation method thereof and application thereof in medicaments, and specifically relates to a thiofuran derivative which is a structural compound shown in formula (I) or a pharmaceutically acceptable salt or optical isomer thereof and a pharmaceutical composition containing the same. The invention also discloses a preparation method of the thiofuran derivative and application of the thiofuran derivative in preparing medicaments for treating thrombotic diseases. The thiofuran derivative compound has good antithrombotic action and high application value in the medicament field.
CA2659693A1 3-substituted-1,5-diarly-2-alkyl-pyrroles highly selective and orally effective cox-2 inhibitors This invention relates to 3-substituted-l, 5-diaryl-2-alkyl- pyrroles of Formula (I), pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and - 5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsul- phonyl-phenyl or with 4-aminosulphonly-phenyl groups.
WO2008134036A1 ALPHA-SUBSTITUTED ARYLMETHYL PIPERAZINE PYRAZOLO[1,5-α]PYRIMIDINE AMIDE DERIVATIVES Derivatives of pyrazolopyrimidine compounds represented by Formula (I) are disclosed. These pyrazolopyrimidine derivatives and pharmaceutical compositions comprising these derivatives are useful in the treatment of HIV mediated diseases and conditions.
CN102827187A Fluoroquinolone acetal isoniazone, and preparation method and application thereof The invention discloses a fluoroquinolone acetal isoniazone, of which the chemical structure general formula is disclosed as Formula I, wherein R1 is hydrogen atom or methyl group; R2 is hydrogen atom or amino group; R3 is hydrogen atom, methyl group, ethyl group, formacyl group, acetyl group, aroyl group or sulfonyl group; R4 is hydrogen atom or methyl group; and X is oxygen atom or sulfur atom. The fluoroquinolone isoniazone disclosed by the invention implements complementarity between the two anti-tuberculosis medicines fluoroquinolone and the isoniazide, lowers the toxic and side effect of the fluoroquinolone and the isoniazide, reduces the generation probability of drug resistance of Mycobacterium tuberculosis for the double-effect antimicrobial agent, and can be used as an anti-Mycobacterium tuberculosis medicine for brand-new structure development of medicinal active substances.
CN102885760A Hydrobromic acid galanthamine controlled-release dry suspension and preparation method thereof The invention relates to a hydrobromic acid galanthamine controlled-release dry suspension and a preparation method thereof. The hydrobromic acid galanthamine controlled-release dry suspension comprises hydrobromic acid galanthamine controlled-release particles A and suspension auxiliary particles B, wherein the diameter of the hydrobromic acid galanthamine controlled-release particles A is 0.05mm-0.6mm, preferably 0.1-0.3mm, and the diameter of the suspension auxiliary particles B is 0.1-0.5mm. The hydrobromic acid galanthamine controlled-release dry suspension is taken once every day and has the grate positive significance in clinical treatment. The suspension auxiliary particles B are skillfully used, so that the technical difficulty of incapability of preparing the hydrobromic acid galanthamine controlled-release dry suspension in the prior art is overcome.
US8003645 type II diabetes; 6-Ethyl-N,N'-bis(3-hydroxyphenyl)-1,3,5-triazine-2,4-diamine; suppress the fall in MTT reduction capacity by beta -amyloid protein; inhibit impairment of long-term potentiation of hippocampal nerve cells, pyrimidine or 1,3,5 triazine derivatives The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
WO2009093761A1 Medicinal composition for inhibiting amyloid-β protein deposition Provided is a medicinal composition for inhibiting amyloid-β protein deposition which comprises a compound represented by formula (I) or a pharmaceutically acceptable salt thereof as the active ingredient. Also provided is a method for inhibiting amyloid-β protein deposition which comprises a step of administering an effective amount of a compound represented by formula (I) or a pharmaceutically acceptable salt thereof to a mammal that is likely diagnosed as having a disease associated with amyloid-β protein. (I)
WO2014058947A1 Compositions and methods for treating cancer using pi3k inhibitor and anti-cd19 maytansinoid immunoconjugate Compositions and methods comprising inhibitors of the phosphoinositide 3-kinase (PI3K) pathway and anti-CD19 maytansinoid immunoconjugates are provided.
US20110070169 Effervescent Oral Fentanyl Dosage Form and Methods of Administering Fentanyl Fentanyl-containing dosage forms and methods using same are described. These dosage forms include substantially less fentanyl by weight than known oral formulation and have advantages in terms of reduced cost and reduced side effects. These dosage forms are intended for oral administration of fentanyl across the oral mucosa.
EP2686318A1 Pyrrolopyridineamino derivatives as mps1 inhibitors The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as "PPA derivatives"), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1-also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I)
CN102286065B Novel abietane-type diterpene derivative as well as preparation method and application thereof The invention relates to an abietane-type diterpene derivative shown as a general formula (I) as well as a preparation method and application thereof to the preparation of medicaments for treating tumors, particularly tumors on a reproductive system.
CN1907432A Application of polysaccharide from the Gastrodia elata Blume in health caring stuff and medicine The invention relates to a gastrodia elata polysaccharide which is a kind of polysaccharide compound extracted by treating gastrodia elata with water lift alcohol deposition method, wherein using gastrodia elata polysaccharide to test the CC14 mice liver hurt, to prove that said gastrodia elata polysaccharide has significant effect on liver protection, to be used in clinic liver treatment.
CN101735265A Therapeutic anti-tumor compound The invention provides a compound or a pharmaceutical salt thereof of formula (I) R1-O-(CH2)nO-L, wherein R1 represents a combretastatin type compound containing non-hydroxyl part, n is 1 to 10, and L represents CO-alkyl carboxylic acid, amino acid residues, phosphoryl or phosphoryl derivatives. The compound of the invention is used for in treatment of anti-tumor medicaments and has high water solubility.
CN101348493B High-purity medicament and preparation thereof The invention provides a method for preparing a high purity drug, particularly relating to a method for preparing high purity cefoperazone sodium or tazobactam sodium. The invention also provides a method for preparing a compound powder-injection of high purity cefoperazone sodium and high purity tazobactam sodium and the high purity drug or high purity drug compound prepared according to the methods.
CN103083280A Vitamin C soft capsules The invention relates to soft capsules, in particular to capsules containing a vitamin C inclusion.
US20110263544 1-Phenylpyrrole Derivatives The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a hydroxy-C1-C4 alkyl group and the like; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like, —R5 represents a sulfamoyl group or a C1-C3 alkylsulfonyl group; R6 represents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing.
CN101829068A Water soluble medicament sustained-release tablets and preparation method thereof The invention discloses water soluble medicament sustained-release tablets, which comprise the following components in part by weight: water soluble medicament 1-30, octadecanol 5-70, Eudragite L 100-55 2-50, talcpowder 2-30 and lactose 2-30. The water soluble medicament may be galanthamine hydrobromide, captopril, metoprolol tartaric acid or pseudoephedrine hydrochloride. In the invention, the octadecanol serving as a hydrophobic auxiliary material and the Eudragite L 100-55 sreving as a water soluble polymer auxiliary are adopted, so the release speed of the medicament can be controlled properly. The Eudragite L 100-55 is insoluble in gastric juice, but dissolves in duodenal juice to make high-viscosity sticky liquid, and thus the release and diffusion speed of the medicament can be reduced. The talcpowder which is a hydrophilic matter insoluble in water plays a porogen role in the sustained-release tablets. In the invention, the release speed of the medicament is regulated by regulating the mixing ratio of the medicament to the auxiliary material. Thus, the release speed of an active medicament is controlled.
US20080124413 Novel composition containing extracts of butyrospermum parkii and the use of such a composition for preparing a medicament or a dietary supplement for the treatment or prevention of inflammation hypersensitivity or pain The present invention relates to a composition comprising an extract or a concentrate of Butyrospermum parkii as a dietary supplement or a pharmaceutical composition and to the use of such compositions for the preparation of a medicament or a dietary supplement for the suppression of hypersensitivity and/or inflammatory reaction. The composition may optionally be formulated with a pharmaceutically acceptable carrier for systemic or topical administration. More specifically, the invention relates to a dietary supplement or a pharmaceutical composition comprising an extract or a concentrate of Butyrospermum parkii, wherein said extract or concentrate contains Butyrospermum-triterpenes and optionally the sterols stigmasterol, avanasterol, 24-methyl-cholest-7-enol, karitesterol A, karitesterol B and α-spinasterol.
WO2013161993A1 Trans-2-decenoic acid derivative and drug containing same The present invention pertains to: a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof; and a drug containing the compound as the active ingredient. Specifically, the trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof is represented by general formula (I) (in the formula, X indicates a substituent group such as 1-pyrrolidilyl, 3-thiazolidyl, or piperidino), and is highly useful as a drug such as a prevention or treatment agent for peripheral nerve disorders resulting from anti-cancer drug administration, a prevention or treatment agent for neurodegenerative disorders or psychiatric disorders including dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, and autism spectrum disorders, a treatment or repair agent for spinal injuries, an analgesic for various pain disorders, and the like.
WO2009157628A1 Pharmaceutical composition for treating or preventing cancer comprising triazine compound as an active ingredient This invention relates to a pharmaceutical composition for anti-cancer. The present invention provides a pharmaceutical composition for anti-cancer comprising any one of triazine compounds represented by a formula I as an active ingredient. The triazine compound as an active ingredient of the pharmaceutical composition in the present invention has an inhibitory activity on cancer cell invasion or a specific cytotoxicity to cancer cells, enabling to be applied as an effective anti-cancer drug.
EP2340249A1 Poly-heteroaryl derivatives for the treatment of cancer The present invention relates to Penta- hexa-, hepta-, octa-, nona- and, deca-heteroaryl derivatives, comprising a combination of heterocycle 1 (Het-1)a and/or heterocycie 2 (Het-2)b and/ or heterocycle 3 (Het-3)c and/or heterocycle 4 (Het-4)d of formulae I, II, III and IV respectively, the N-oxides, the pharmaceutically acceptable addition salts. The compounds claimed are suitable for the treatment of cancer.
US7582659 effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci; 1-[5(R)-3-[4-[2-[(1 alpha ,5 alpha ,6 beta )-6-Cyano-3-azabicyclo[3.1.0]hexan-6-yl]pyridin-5-yl]-3-fluorophenyl]-2-oxooxazolidin-5-ylmethyl]-1,2,3-triazole; side effect reduction This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.
WO2012103015A2 Extended-release beta agonist/steroid transdermal patches and methods for using the same Extended-release beta agonist/steroidal transdermal patches are provided. Transdermal patches of embodiments of the invention have an adhesive matrix which includes both a beta agonist, e.g., tulobuterol, and steroid, e.g., dexamethasone, where the matrix is configured to be storage-stable and provide for extended release of the beta agonist and steroid. Aspects of the invention further include methods of using the transdermal patches, e.g., in the treatment of pulmonary conditions, such as asthma.
EP1931334A2 Functionalized drugs and polymers derived therefrom Compounds selected from: formula (I) where DRUG-OH, DRUG-COOH and DRUG-NH2 are biologically active compounds; each X is independently selected from -CH2COO- (glycolic acid moiety), -CH(CH3)COO- (lactic acid moiety), -CH2CH2OCH2COO- (dioxanone moiety), -CH2CH2CH2CH2CH2COO- (caprolactone moiety), -(CH2)yCOO-, where y is 2-4 or 6-24 and -( CH2CH2O)ZCH2COO-, where z is 2-24; each Y is independently selected from -COCH2O- (glycolic ester moiety), -COCH(CH3)O- (lactic ester moiety), -COCH2OCH2CH2O- (dioxanone ester moiety), -COCH2CH2CH2CH2CH2O- (caprolactone ester moiety), -CO(CH2)mO-, where m is 2-4 or 6-24 and -COCH2O(CH2CH2O)n- where n is between 2-24; R' is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; and p is 1-6. Multi-functional compounds and drug dimers, oligomers and polymers are also disclosed.
CN1879636A Application of oligosaccharide in preparation of medicine for treating hyperacute rejection The invention relates to the application of oligosaccharide in the hyperacute rejection medicine caused by anti-swine-human special organ implantation, wherein said oligosaccharide can be stachyose or verbascose; the prepared medicine comprises medicine shaping agent or carrier allowed by said agent; the invention selects small molecular compound oligosaccharide, to combine the natural antibody preset in human body, to avoid antibody combining with the antigen at the surface of swine surface to caused hyperacute rejection. The oligosaccharide can be extracted in batch, iwht low cost, while it can restrain the generation of hyperacute rejection, without reducing immunity of human body.
US7737144 1-Ethyl-6-methyl-3-phenyl-1H-pyrinido[5,4-e]1,2,4]triazine-5,7-dione, used for lowering blood sugar, treating non-insulin dependent diabetes and insulin resistance; antidiabetic agents The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diones, pharmaceutically acceptable salts thereof and physiologically functional derivatives. The invention therefore relates to compounds of the formula I, in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are suitable for use as antidiabetics, for example.
US20120022167 Trans-Clomiphene for Metabolic Syndrome The present invention relates to the administration of compositions comprising an antiestrogen, preferably trans-clomiphene, for treating metabolic syndrome in a subject. The invention is also directed to methods for reducing fasting glucose levels in a subject by administering a composition comprising an antiestrogen, preferably trans-clomiphene.
WO2009155135A1 Composition comprising liposome-entrapped doxorubicin and methods of admnistration for treatment of multiple myeloma Methods and pharmaceutical compositions are disclosed for treating subjects with relapsed multiple myeloma who have been previously treated with a peptide boronic acid compound by administering an effective combined amount of a liposome-entrapped doxorubicin and a peptide boronic acid compound. In one embodiment, methods and pharmaceutical compositions are disclosed for treating subjects with relapsed multiple myeloma who have been previously treated with bortezomib by administering an effective combined amount of the liposome-entrapped doxorubicin product identified by the tradename DOXIL® and bortezomib.
US6869622 Extracts of the root of a plant of the family Valerianacae for use in therapy of sleep disorders A pharmaceutical composition comprising extracts of the root of a plant of the family Valerianacae, and methods of using such composition and/or extracts of the root of a plant of the family Valerianacae to improve sleep quality and sleep efficiency and to improve sleep structure and sleep architecture, are described. Sleep quality, sleep efficiency, sleep structure and sleep architecture may be in the context of various criteria or parameters, as described herein. Specifically, a pharmaceutical composition that reduces wake after sleep onset, increases total sleep time, increases sleep efficiency, and/or increases sleep time spent in sleep stages three and four, in a normal adult is described, the composition comprising therapeutically effective amounts of valerenic acid and its derivatives, kessane derivatives, valeranone, valerenal, and amino acids. The composition may be prepared by the steps of (i) adding the roots to an alcoholic extraction solvent to form a mixture, wherein the alcoholic extraction solvent comprises between approximately 50% (v/v) to approximately 100% (v/v) ethanol in a remainder of water, and (ii) heating the mixture to a temperature of between approximately 70° C. to approximately 80° C. for a period of at least two hours; wherein valerenic acid is present in the extract, the content of valepotriates in the extract is substantially reduced with respect to its content in the root, and the content of valerenic acids in the extract is not substantially reduced with respect to its content in the root; and minimizing the yield of unstable valepotriates. The valerenic acid derivative, where present, is preferably selected from acetoxyvalerenic acid, hydroxyvalerenic acid, valerenal, valerenol.
US20100063583 Use of soluble epoxide hydrolase inhibitors in the treatment of inflammatory vascular diseases Disclosed herein are compositions and methods for treating inflammatory vascular diseases. Examples of inflammatory vascular disease include, but are not limited to, in-stent stenosis, coronary arterial diseases (CAD), angina, acute myocardial infarction, acute coronary syndrome, chronic heart failure (CHF), peripheral arterial occlusive diseases (PAOD), critical limb ischemia (CLI), cardiac, kidney, liver and intestinal ischemia, renal failure, cardiac hypertrophy, atherosclerosis, abdominal aortic aneurysm, vasculitis, carotid artery stenosis.
WO2012153884A1 Composition having improved stability for ameliorating acne The present invention provides a composition for preventing or treating acne, comprising: benzoyl peroxide, a derivative thereof, a hydrous form thereof or pharmaceutically acceptable salts thereof; clindamycin, a derivative thereof, a hydrous form thereof or pharmaceutically acceptable salts thereof; and sodium pyrosulfite. The composition has high stability due to inclusion of sodium pyrosulfite. Also, said composition includes pulverized benzoyl peroxide, thereby providing high stability and an excellent perception of utility.
EP2170873B1 Isoxazole-imidazole derivatives The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula (I): wherein R1, R2 and R3 are as described in the specification.
CN102846635A Inhalant containing N-acetyl-L-cysteine and mometasone furoate and preparation method thereof The invention relates to an inhalant containing N-acetyl-L-cysteine and mometasone furoate and preparation method thereof. The inhalant is composed of mometasone furoate and N-acetyl-L-cysteine as the active ingredients, and one or more pharmaceutical adjuvants suitable for inhalation drug delivery.
CN102600301A Simple and efficient dermatophytosis treatment liquid medicine prescription The invention provides a dermatophytosis treatment liquid medicine prescription with simple prescription, easy availability, simple use, and good effects of dermatophytosis treatment, foot odor removal, blood circulation and skin care. The liquid medicine mainly comprises tea leaves, distilled water, edible salt and the like, after the prescription is used in a patient for 3 to 5 days, a serious wound is not cracked any more, the skin is softened, and necrosis skin naturally falls off, and the rest skin becomes smooth; and a slight wound is gradually recovered, and skin feels comfortable and becomes smooth as before. The prescription has the advantages of simple acquiring, preparing and using processes, and excellent treatment effect.
EP2386543A1 3-Z-[1-(4-(n-((4-methyl-piperazin-1-yl)-methylcarbonyl)-n-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate and the use thereof as a pharmaceutical composition The present invention relates to the compound 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate of formula I and the use thereof as a pharmaceutical composition.
WO2007126020A1 Compound having activity of blocking nmda receptor channel, and pharmaceutical agent using the same [PROBLEMS] To provide a novel compound having an activity of blocking an NMDA receptor channel, and also provide a pharmaceutical agent comprising the compound. [MEANS FOR SOLVING PROBLEMS] A pharmaceutical agent for the treatment or prevention of a disease induced by supranormal excitability of an NMDA receptor, which comprises a compound having an activity of blocking an NMDA receptor channel and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt. (1)
CN101336884A Preparation method of microelement nano fibrofelt The invention relates to a method for preparing nano-sized fiber felt containing trace elements. The method comprises the following steps: (1) mixing trace element nanoparticles or trace element compounds with a solvent, adding a polymer under stirring, stirring for swelling for 4 hours, and degassing for 15 minutes by an ultrasonic processor to obtain a spinning stock liquid; and (2) pouring the spinning stock liquid into a liquid container, carrying out the electrostatic spinning using a subdued syringe needle as the capillary tube for stream spraying, under such conditions that the flow speed is in the range of 1.0 mL*h<-1> to 3.0mL*h<-1>, the distance between the receiving plate to the nozzle is in the range of 10cm to 30cm, the voltage is in the range of 10kV to 30kV, the environmental temperature is in the range of 15 DEG C to 40 DEG C and the ambient humidity is in the range of 50% to 75%, and vacuum-drying for 24 hours at the room temperature to obtain the final nano-sized fiber felt. The preparation method has the advantages of simple process and suitability for industrialized production. The produced nano-sized fiber felt loads the trace elements necessary for the human body and can be further processed to oral, transdermal or transmucosal administration system for human beings, or processed to feed additive for nutrient supplementation in animal husbandry.
EP2535059A1 Use of compound binding to msin3b that specifically binds to neuron restrictive silencer factor (nrsf) The present invention identifies a compound which binds to the PAH1 domain of mSin3B that specifically binds to neural restrictive silencer factor NRSF, and uses the compound as a prophylactic and/or a therapeutic for diseases associated with abnormal expression of neural restrictive silencer factor NRSF/REST or abnormal expression of genes targeted by NRSF/REST, such as Huntington's disease, medulloblastoma and neuropathic pain. The present invention provides a pharmaceutical composition comprising a substance capable of binding to the PAH1 domain of mSin3B, e.g., a compound represented by the following formula (I), a pharmacologically acceptable salt thereof, or a pharmacologically acceptable ester thereof: wherein n represents 0 or 1; R1, R2, R3, R4 and R5 each independently represent a hydrogen atom, a hydrocarbon group or a functional group; Y represents a single bond, a carbonyl group, -CONH-, -NHCO- or a sulfonyl group; and Z represents a nitrogen-containing heterocyclic group which may have a substituent, an amino group which may have a hydrocarbon group or an aromatic hydrocarbon group, or a nitrogen and oxygen-containing heterocyclic group which may have a substituent.
EP1809607A1 Sulfonyl benzimidazole derivatives This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, GERD, constipation, diarrhea, functional gastrointestinal disorders, irritable bowel syndrome, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, COPD, cryptogenic fibrosing alveolitis and bronchitis.
US20080096912 Indole, azaindole and related heterocyclic pyrrolidine derivatives This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
US8058441 For control fertility, contraception, breast cancer, prostate cancer and endometriosis; modulating activity of the follicle stimulating hormone (FSH) receptor; 1-Acetyl-6-(tert-butoxycarbonyl)amino-4-phenyl-1,2,3,4-tetrahydro-2,2,4-trimethylquinoline The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is (CO)—O, (SO)2—O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2—NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (6-10C)aryl, (3-9C)heteroaryl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, (1-4C)(di)alkylamino(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkylthio(1-4C)alkyl, (1-4C)alkylcarbonylamino(1-4C)alkyl, (1-4C)alkoxycarbonyl(1-4C)alkyl, (1-4C)alkoxycarbonylamino(1-4C)alkyl, (3-6C)cycloalkyl, (2-6C)heterocycloylkyl, or R8 and R9 may be joined in a (2-6C)heterocycloalkyl ring. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to control fertility.
WO2008044731A1 N-phenyloxamidic acid derivative Disclosed is a compound represented by the general formula (I) below, which has a plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, a salt thereof, or a hydrate or solvate of any of them. (I) (In the formula, R1 represents a C6-10 aryl group or a C6-10 aryl group substituted with a group selected from the group consisting of a halogen atom, a cyano group, a nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group and a C1-6 alkylsulfanyl group; R2 represents a C6-10 aryl group or a C6-10 aryl group substituted with a group selected from the group consisting of a halogen atom, a hydroxy group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a C1-6 alkylsulfanyl group and a phenyl group; X represents a single bond or an oxygen atom; Z represents a phenylene group or a substituted phenylene group; and m represents 0 or 1.)
EP1492774A2 Pyrimidone derivatives useful for the treatment of inflammation and immunological diseases AbstractThe present invention relates to novel pyrimidone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel pyrimidone derivatives of the general formula (I).
CN103446144A Application of Lycojaponicumin C in biliary duct cancer treatment drug The invention discloses application of Lycojaponicumin C in preparation of a biliary duct cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Lycojaponicumin C also has remarkable inhabiting effect on growth of A human biliary duct cancer cell strain RBE. Therefore, the Lycojaponicumin C can be used for preparation of an anti-biliary duct cancer drug and has good development and application prospect. The application of the Lycojaponicumin C in the preparation of the biliary duct cancer treatment drug is disclosed for the first time. Due to the fact that the fact that the skeleton type is a novel skeleton type, and the high biliary duct cancer cell inhibiting activity of the Lycojaponicumin C is previously unimagined.
CN103450321A Nortriterpene compound as well asand preparation method and application thereof The invention discloses a nortriterpene compound as well asand a preparation method and an application thereof. The preparation method comprises the following steps: (1) drying and crushing stems and branches of elderberry, heating the stems and branches by 40-80% ethanol and carrying out reflux extraction for 1-3 times, combining an extracting liquids and drying to obtain elderberry extract powder; suspending with an appropriate amount of water, and sequentially gradient-eluting with water, 30% ethanol-water, 40-60% ethanol-water and 90-100% ethanol-water to obtain a water-eluting part, a 30% ethanol-water eluting part, a 40-60% ethanol-water eluting part and a 90-100% ethanol-water eluting part through D101 macroporous resin column chromatography separation; (2) combining the 40-60% ethanol-water eluting part and the 90-100% ethanol-water eluting part in the step (1), and preparing the compound disclosed by the invention sequentially through ODS (Octadecyl Silane) column chromatography, ODS medium- and low-pressure columns, Sephadex LH-20 column chromatography separation and high performance liquid chromatography. The compound disclosed by invention can be used for treating liver tumor diseases.
WO2006081771A1 Artemisine (qinghaosu) derivatives, their preparation methods and their use, and pharmaceutical compositions containing the same The invention provides a artemisine derivative of the following formula I, its preparation method and use, as well as a pharmaceutical composition containing such artemisine derivative and its use. The artemisinin derivatives of the present invetion and the pharmaceutical compositions containing the same have immunosuppressive activities and can be used safely. The compositions which comprise the artemisine derivatives can be made into long-term dosage forms such as tablet, pellet and the like, and have widely productive and use value.
US20100166737 P38Alpha as a Therapeutic Target in Bladder Carcinoma The present invention concerns methods and compositions for treating bladder carcinoma by p38 inhibitors.
WO2012136772A1 Fused pyrrole derivates as estrogen receptor ligands The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein Z, A, B, D, E, G, M1, M2, M3, M4, M5, M6, p, q, r, R3, R4, R5 and R6 are as defined in the specification. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
US20050249761 Topical composition comprising at least one aryl oxime and bisabolol The invention relates to a topical composition comprising at least one aryl oxime and bisabolol, to a mixture suitable for the preparation of the topical composition comprising at least one aryl oxime and bisabolol, and to a process for the preparation of this topical composition.
CN101406515A Breast perfusate for treating mammitis of milk cattle and preparation thereof The invention relates to the field of veterinary medicine for treating bovine mastitis. Antibiotic is mainly adopted for treating bovine mastitis currently, slowly takes effect, has poor curative effect, large stimulation on milk cows and large antibiotic residue in latex, and is harmful to the human body. In order to solve the problems, total tanshinone and alizarin are dissolved in ethanol, added with tween-80 for grinding, added with a mixture of carbomer and matrine for grinding after full grinding, and added with lactic acid to adjust the pH value after full grinding; and a liquid medicine is grinded for 30 minutes in a colloid mill, and subjected to filling and steam flowing sterilization to prepare prefusate. The prefusate obtained has the functions of inhibiting the growth of pathogens such as Staphylococcus aureus, streptococcus dysgalactiae, colon bacillus and so on in affected parts, clearing away heat and expelling superficial evils, killing bacteria and diminishing inflammation, increasing blood flow, and preventing blood sludging, achieves the effects of clearing out the pus, reducing edema and promoting blood circulation by removing blood stasis, and simultaneously has the characteristics of simple preparation technology, low cost, easily controlled quality and no antibiotic residue in the latex.
CN103462989A Application of Lycojaponicumin B in preparation of medicines for resisting human body fungi The invention relates to an application of Lycojaponicumin B in the preparation of medicines for resisting human body fungi, belonging to the field of medicines. The Lycojaponicumin B has very strong inhibitory effect on trichophyton rubrum, microsporum lanosum or trichophyton tonsurans. Therefore, the Lycojaponicumin B can serve as a compound capable of resisting human body fungi and is expected to be applied in the preparation of related medicines. The application of the Lycojaponicumin B in the preparation of the medicines for resisting human body fungi is disclosed for the first time. As the skeleton type of the Lycojaponicumin B belongs to a brand-new skeleton type, the Lycojaponicumin B has unexpected strong inhibitory activity on human body fungi, and the possibility that other compounds provide revelation does not exist. The Lycojaponicumin B has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for preventing and treating human body fungi infection.
CN101683516A Pharmaceutical composition for treating injuries from falls and rheumatism and preparation method thereof The invention discloses a pharmaceutical composition for treating injuries from falls and rheumatism and a preparation method thereof. The pharmaceutical composition is prepared from the following rawmedicines: radix aconiti, myrrh, radix clematidis, Rhizoma Zingiberis, Eupatorium japonicum, cassia, borneol, musk and the like. The pharmaceutical composition can be prepared into clinically acceptable preparation formulations by adding pharmaceutically conventional auxiliary materials according to conventional techniques. The pharmaceutical composition has the effects of activating meridians and collaterals, promoting the blood circulation to remove blood stasis, removing the turgidity to relieve pains, expelling the wind-evil, removing the wetness, eliminating the cold, softening hard lumps and dispelling nodes. The pharmaceutical composition has obvious functions for treating injuries from falls, pains from anemofrigid-damp arthralgia in the parts (joints) of the whole body, hyperosteogeny, ankylosing spondylitis, cough due to wind-cold evil, bronchitis, women's algomenorrhea and other persistent ailments with pains.
CN1590396A Picrorhiza total glycoside extract and its application in preparation of liver disease medicine and preparation method A picroside is prepared through extracting from picrorhiza, filtering, resin adsorption and washing for removing impurities, eluting, vacuum concentrating, drying and pulverizing. It can be used to prepare the medicines in the oral-taken form or the form of injection for preventing and treating hepatism. The picrosid content can reach 90%.
CN101766697A Antifungal medicament for treating skin tinea and preparation method thereof The invention discloses an antifungal medicament for treating skin tinea and a preparation method thereof. The medicament mainly comprises sweet wormwood volatile oil, divaricatus and rhubarb as raw materials to prepare effective components, and a pharmaceutically acceptable vector is added to prepare the medicament for external use. The medicament and the manufacturing method of the invention are unique, have a wide antifungal spectrum, obtain good curative effects for treating tinea capitis, tinea corporis, tinea cruris, tinea manuum, tinea pedis, tinea unguium and senile pruritus through clinical experiments, and have no toxic side effects on a human body and viscera.
WO2013155422A1 Methods of treating alopecia and acne Method of treating alopecia and acne with are disclosed. The compounds fall within described by formula I or II:
CN101336925A Use of PS-341 in preparing medicine for synergistic inductive differentiation therapy of leukaemia The invention aims to provides an application of a compound PS-341 in preparing medicaments for cooperating with and promoting retinoid drugs to induce differentiation of leukemia cells so as to treating leukemia. The PS-341 (bortezomib) is a proteasome inhibitor with a molecular formula of C19H25BN4)4, the concentration of the PS-341 is 1*10<-10>-1*10<-8>M, and the concentration of a retinoid drug is 1*10<-9>-1*10<-5>M. The compound PS-341 can distinctly promote the inhibitory action of the retinoid drug on the proliferation of leukemia cells and promote the expression of a leukemia cells differentiation surface specific antigen CD11b, so that the nuclear cytoplasmic ratio is decreased, and the count of segmented cells is distinctly increased compared with the single retinoid drug group. The action of the compound PS-341 in promoting the retinoid drug to induce differentiation of leukemia cells has distinct concentration and time dependence. The invention opens up a new drug application field of the compound PS-341.
CN103638131A Medicine for treating mycotic stomatitis The invention discloses an external medicine for treating mycotic stomatitis. The medicine is a medicine composition which is prepared by taking pure natural plant, mineral and other substances as raw materials through a certain process. The medicine comprises the following components: calcined gypsum, borax, dandelion, indigo naturalis, rhizoma coptidis from Sichuan of China, frankincense, myrrh, cinnabar and borneol. Due to a large number of clinical applications, the medicine is high in curative effect, has no toxic and side effect and has no recurrence after healing. The medicine is extensive in sources of raw materials, low in cost and simple in preparation method; three wastes (waste gas, waste water and waste residues) are not discharged in production of the medicine; the effective rate is 100%; the cure rate is 98.6%.
CN103372048A Medicament for treating fire burn The invention discloses a medicament for treating a fire burn, relates to a medicament for treating the fire burn, and provides a medicament for treating the fire burn capable of effectively relieving pain caused by I and II cauma, and preventing wound infection. Large-leaf acanthopanax, red laoxiongbao (Chinese character), and cat claw stab are decocted by water for three times, and filtered; filtrate is merged, and concentrated to 2/3 to heat a little; tablets and berberine hydrochloride are added to agitate and dissolve.
US20090247535 Use of ranolazine for non-cardiovascular disorders Disclosed is a method of treating a non-cardiovascular disorder characterized by an abnormal persistent sodium current in a subject in need of treatment thereof, said method comprising administering to the subject an effective amount of a compound of Formula (I): wherein: m is 1 or 2; R1, R2, R3, R4, and R5 are each independently selected from the group consisting of hydrogen, halo, CF3, CN, OR22, SR22, N(R22)2, S(=O)R22, SO2N(R22)2, C(═O)R22, alkylamido, alkyl, alkenyl, morpholino, and pyrrolyl, wherein the alkyl substituent is optionally substituted with one substituent selected from the group consisting of OR22, or R2 and R3 together or R4 and R5 together can be alkylene; R6, R7, and R8 are each independently selected from the group consisting of H and alkyl; R9, R10, R11, R12, R13, R14, R15, and R16 are each independently selected from the group consisting of H and alkyl, or wherein one or more of R9 and R10, R11 and R12, R13 and R14, and R15 and R16 are together ═O; R17, R18, R19, R20 and R21 are each independently selected from the group consisting of H, halo, OR22, alkyl, and aryl; X is O or S; and R22 is selected from the group consisting of H and alkyl; or a pharmaceutically acceptable salt or a pharmaceutically acceptable ester thereof. The disorder can be epilepsy.
US20080146557 Vasopressin (V1a) receptor; dysmenorrhea, hypertension, chronic heart failure, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders; 1'-[(1-benzyl-2-methyl-1H-indol-3-yl)carbonyl]spiro[indene-1,4'-piperidine] one for example The invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the spiro-piperidine head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, methods for preparing the compounds and pharmaceutical compositions, and their use in the treatment of dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxious and depressive disorders.
CN1739558A Dietotherapeutic product for preventing and treating primary and secondary urate calculi, gout and acalcerosis and its prepn process The dietotherapeutic product for preventing and treating primary and secondary urate calculi, gout and acalcerosis consists of salt of organic acid, salt of inorganic acid, nucleotide, vitamin and trace elements. The dietotherapeutic product operates on that the product creates conditions for dissolving urate in water soluble alkali salt and removing and for dissolving calcium salt in acid solution for being absorbed and utilized, the nucleotide avoids purine to synthesize urate, and the vitamin and the trace elements reinforce the activity of enzyme, protect the functions of cell and organ, recover nucleotide and make purine to synthesize essential nucleic acid to reduce purine and urate and avoid urate calculi and gout. The dietotherapeutic product has obvious curative effect, no toxic side effect, simple preparation process, and low cost.
EP2714006A1 Intranasal testosterone bio-adhesive gel formulations and use thereof for treating male hypogonadism The present invention relates to pernasal testosterone bio-adhesive gel formulations for intranasal administration and testosterone replacement treatment methods for using the pernasal testosterone bio-adhesive gel formulations for providing sustained intranasal delivery of testosterone to testosterone deficient males to treat, for example, male subjects diagnosed with hypogonadism.
CN103690539A Application of koumine and koumine homolog in preparation of medicines for treating diabetic complications The invention discloses an application of koumine and koumine homolog in the preparation of medicines for treating diabetic complications. The koumine is high in therapeutic index, the therapeutic index of the koumine for treating the pain hypersensitivity of diabetic rats is estimated to reach 4762, the koumine can be used for obviously improving the neuropathy of the diabetic rats, the details are explained in the embodiment 1, and the koumine is large in safe therapeutic window and suitable for the preparation of the medicines for treating the diabetic complications, is likely to have no tolerance or addiction, and has low side effects, and therefore, the koumine has potentially great economic effect. The koumine and the koumine homolog or pharmaceutically acceptable salts of the koumine can be applied to the preparation of the medicines for treating the diabetic complications, have no disadvantages of two types of clinically frequently-used medicines for treating the diabetic complications, are developed and researched according to national specifications about innovative drug examination and approval and are expected to be prepared into the novel national class-1 medicines for treating the diabetic complications which are capable of effectively treating the diabetic complications, have small side effects, clear industrialization prospect, no tolerance and no addiction and possess the national proprietary intellectual property rights.
US6916485 Mixture of protein, hydrophilic polymer, group 1a alkyl sulfate and sugar The present invention concerns a prolonged release bioadhesive mucosal therapeutic system containing at least one active principle, with an active dissolution test of more than 70% over 8 hours and to a method for its preparation. The bioadhesive therapeutic system may be in tablet form and may contain quantities of natural proteins representing at least 50% by weight of active principle and at least 20% by weight of the tablet, between 10% and 20% of a hydrophilic polymer, and compression excipients, and may contain between 4% and 10% of an alkali metal alkylsulphate to reinforce the local availability of active principle and between 0.1% and 1% of a monohydrate sugar.
US7378518 Vascular conditions such as atherosclerosis, hypercholesterolemia, diabetes, obesity, stroke, demyelination; lowering plasma levels of sterols and/or stanols The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating vascular conditions, such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols.
CN101336922A Rosuvastatin amlodipine composition A pharmaceutical composition is an organic salt formed by an organic acid rosuvastatin and an organic base amlodipine with a molar ratio of 1:1. The pharmaceutical composition can be made into any dosage forms together with a pharmaceutically-acceptable carrier for reducing blood pressure and blood lipid, reducing myocardial infarction and treating cerebral apoplexy. The inventive pharmaceutical composition has the advantages of stable physiochemical indexes, controllable product quality, and convenient administration.
CN102824329A Adefovir dipivoxil liquid capsules and preparation method thereof The invention relates to adefovir dipivoxil liquid capsules and a preparation method thereof. The adefovir dipivoxil liquid capsules comprise adefovir dipivoxil and pharmaceutically acceptable plant oil. The capsule shell material of the liquid capsules is a pharmaceutically acceptable capsule non-gelatin shell material. An annular sealing material is coated on the fitting positions of the liquid capsules. The invention also discloses a preparation method of the adefovir dipivoxil liquid capsules. The adefovir dipivoxil liquid capsules provided by the invention have an advantage of high stability. With the adefovir dipivoxil liquid capsule preparation method provided by the invention, the prepared liquid capsules are more stable. The method is scientific, reasonable, and time-saving. The method has the advantages of high efficiency, low cost, and low pollution to the environment.
CN101069700A Composition for preventing manmmal vagina infection and use The present invention relates to a medicine composition for curing human and animal vaginal infection. Said medicine composition includes probiotics capable of producing beta-hydroxy-propionaldehyde (beta-HPA), glycerine, beta-hydroxypropionaldehyde and natamycin. The invented medicine composition can inhibit and kill various vaginal pathogenic bacteria and fungi.
WO2011049677A1 Compounds and compositions as tlr activity modulators The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.
US20090312289 Ibandronate polymorph The present invention relates to a new crystalline polymorph of 3-(N-methyl-N-pentyl)amino-1-hydroxypropane-1,1-diphosphonic acid monosodium salt monohydrate (Ibandronate) with the following formula
CN102093411A Lysine-based compounds The invention provides lysine-based compounds of a formula (I) and pharmaceutically acceptable ammonium salts of the compounds of the formula (I) have amino, wherein R1 may be (OH)2P(O)-, (NaO)2P(O)-, alkylketo or cycloalkylketo; X may be F, Cl and Br; and R2 and R3 are specified in the context. The lysine-based compounds have a unit capable of cracking physiologically, namely R1. Thus, once the unit cracks, a human immunodeficiency virus (HIV) aspartyl protease inhibitor can be released.
US20080207617 Prevent autophosphorylation of tyrosine kinase; therapy for hematopoietic cancer; leukemia; myelodysplastic syndrome An objective of the present invention is to provide compounds and pharmaceuticals useful for the treatment of disease where the inhibition of autophosphorylation of FMS-like tyrosine kinase 3(Flt3) is therapeutically effective. The present invention relates to a pharmaceutical composition for use in the treatment or prevention of diseases where the inhibition of autophosphorylation of Flt3 therapeutically or prophylactically effective, which comprises a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X represents CH or N; Z represents O or S; R1, R2, and R3 represent H, OH, or optionally substituted alkoxy; R4 represents H; R5, R6, R7, and R8 represent H, Hal, alkyl or the like; and R9 represents, e.g., alkyl substituted by t-butyl or the like.
CN102114111A Medicament for treating damp-heat stagnation type acne The invention relates to a medicament using plants as raw materials, in particular to the medicament for treating damp-heat stagnation type acne. The medicament comprises active ingredients and pharmaceutically acceptable excipients, and is characterized in that the active ingredients are prepared by the following active pharmaceutical ingredients by weight percent: 6-12% of artemisia capillaris thunb, 6-12% of baical skullcap root, 11-20% of talc, 6-12% of immature bitter orange, 7-10% of loquat leaf, 8-14% of radix salviae miltiorrhizae, 8-14% of spreading hedyotis herb, 6-10% of common selfheal fruit-spike, 6-10% of red paeony root, 4-7% of Chinese angelica and 4-7% of liquoric root. The active ingredients can be prepared into granules or capsules, thereby having the effects of clearing heat, removing dampness and cooling blood.
US20090304771 Local Delivery System for the Chemotherapeutic Drug Paclitaxel The present invention provides methods for producing a semi-degradable polymeric composite drug delivery device for localized delivery of chemotherapeutic agents to be used in conjunction with total vertebral body replacement surgery that requires placement of a vertebral replacement cage for the treatment of a spinal neoplasm.
US7060686 treating, preventing, or inhibiting disorders associated with inflammation, cell-proliferation, and pain by administering a pseudopterosin, a seco-pseudopterosin, a diterpene aglycone, or a tricyclic diterpene Methods for treating, preventing, or inhibiting diseases and disorders associated with inflammation, cell-proliferation, and pain comprising the administration of a compound having the structural formula wherein R1 is a hydrogen, alkyl, aryl, hydroxyalkyl, cycloalkyl, cycloalkenyl, carboxylic acid, alkylamino or amide group having from 2 to 20 carbon atoms, R2, R3, and R4 are each independently hydrogen or an acyl residue having from 1 to 6 carbon atoms, R5 is hydrogen, CH3, or CH2OH, and R6 is an organo group such as a hydrocarbon having from 1 to 10 carbon atoms are disclosed. Other seco-pseudopterosins and compounds related to pseudopterosins are disclosed.
CA2589561A1 Treatment of neurodegenerative diseases by the use of laptm4a The invention relates to the use of a LAPTM4A-interacting molecule for the preparation of a pharmaceutical composition for the treatment of a neurogenerative disease. Hereby the LAPTM4A-interacting molecule is preferably an inhibitor of LAPTM4A and particularly it has the capacity to modulate the activity of gamma-secretase and/or beta-secretase. Furthermore the invention concerns a process for identifying a gamma-secretase and/or a beta-secretase modulator, comprising the following steps: a. identifying of a LAPTM4A-interacting molecule by determining whether a given test compound is a LAPTM4A-interacting molecule, b. determining whether the LAPTM4A-interacting molecule of step a) is capable of modulating gamma-secretase and/or beta-secretase activity.
US20110028541 Lubiprostone crystal, the use and the method for the preparation thereof The present invention relates to a lubiprostone crystal, the method for the preparation thereof, and a pharmaceutical composition or kit comprising the same, as well as the use of said crystal in the preparation of a medicament for the treatment of gastrointestinal tract diseases, especially constipation. The X-ray powder diffraction pattern of said crystal comprises characteristic peaks measured at the following 2θ reflection angles: 14.6±0.2°, 17.0±0.2° and 19.6±0.2°. As compared to amorphous lubiprostone, the crystal of the present invention has the advantages of relative high purity, stable properties and easy-for-storage and use.
CN101450046B Nizatidine freeze-dried powder injection and preparation method thereof The invention relates to a freeze-dry powder preparation for nizatidine injection and preparing method thereof. The freeze-dry powder is composed of active component nizatidine and pharmaceutically acceptable carrier component, the weight ratio of the nizatidine compound and the selected pharmaceutically acceptable carrier is 1-10:0-10, wherein, the pharmaceutically acceptable carrier is composedof at least one of excipient, latent solvent, antioxidant or water, the excipient is at least one of mannitol, sodium chloride, rheomacrodex, benzoic acid, glucide substance, cyclodextrin, soluble starch, cellulose substance, ascorbic acid, hydrolyzed gelatin, glycine or water, the latent solvent is at least one of aminoacids substance, alcohols substance, acidamides and carbamides derivatives oramines, the antioxidant is at least one of sodium bisulphate, ascorbic acid derivatives aminoacids or chelating agent. The freeze-dry powder preparation prepared by the invention has good stability, simple operating process and ontrollability.
WO2010044685A1 Nitrophenyl mustard alcohols, their corresponding phosphates and their use as targeted cytotoxic agents The invention provides nitrophenyl mustard compounds useful in cancer therapy as targeted cytotoxic agents, of Formula (I) and Formula (II): wherein X represents C1, Br, I, or OSO2R1, Y represents C1, Br, I, or OSO2R1, Z represents at any available ring position -CO- or -SO2-, R represents: (1) a straight or branched chain C1-6 alkyl group or -CH2CH2OMe, when X and Y are the same, or (2) a straight or branched chain C3-6 alkyl group or -CH2CH2OMe when X and Y are different, R1 represents a straight or branched chain C1-6 alkyl group, and n is an integer from 1 to 6; and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, comprising the compounds of Formula (I) and (II), and methods of treating cancer by administration of the compounds.
EP2768478A1 Paste comprising non-steroidal anti-inflammatory An oral paste comprising : (i) at least one non-steroidal anti-inflammatory drug; (ii) at least one viscosity modifying agent; and (iii) a liquid vehicle.
CN103554103A Indole[3,2-c]quinoline compounds or pharmaceutically acceptable salts thereof, and preparation method and application thereof The invention discloses indole[3,2-c]quinoline compounds represented by formula I or pharmaceutically acceptable salts thereof, and a preparation method and an application thereof, and belongs to the technical field of the pharmaceutical chemistry. The indole[3,2-c]quinoline compounds or pharmaceutically acceptable salts thereof have a very good tubercle bacillus resisting activity, and the MIC value of the most compounds is 2.5mug/mL.
US7038046 Triazine derivatives and their use as sunscreens There are described triazine derivatives of formula (1), wherein R1 is an unsubstituted or mono- or poly-hydroxy-, C1-C18 alkyl-, C1-C18 alkoxy-, amino-, C1-C5 monoalkylamino- or di-C1-C5 alkylamino-substituted C1-C18 alkyl, C2-C18 alkenyl, C6-C10 aryl or C6-C10 heteroaryl radical; unsubstituted or C1-C5 alkyl-substituted C5-C7 cycloalkyl or C5-C7 cycloalkenyl; —OR′; or —NR′R″; R2 is hydrogen; an unsubstituted or mono- or poly-hydroxy-, C1-C18 alkoxy-, cyano-, amino, C1-C5 monoalkylamino- or di-C1-C5 alkylamino-substituted C1-C18 alkyl, C2-C18 alkenyl; C6-C10 aryl or C6-C10 heteroaryl radical; —OR′; or —NR′R″; or R1 and R2 together form a 5- to 7-membered carbocyclic or heterocyclic ring; A is C1-C5 alkyl; an unsubstituted or hydroxy-, C1-C18 alkyl- or C1-C18 alkoxy-substituted C6-C10 aryl or heteroaryl radical; or a radical of formula (1a); R′ and R″ are each independently of the other hydrogen; unsubstituted or mono- or poly-hydroxy-, halo-, C1-C18 alkyl-, C1-C18 alkoxy-, amino- or quaternary ammonium group-substituted C1-C18 alkyl, C5-C7 cycloalkyl or phenyl; R3 is hydrogen; or C1-C6 alkyl; and n is 0 or 1. The compounds according to the invention are suitable especially as sun protective agents in cosmetic, pharmaceutical and veterinary medicine preparations
WO2007097470A3 Fused nitrogen- comprising heterocyclic compound A compound of the formula: wherein ring' A is a 7-membered or 8-membered nitrogen- containing ring optionally further substituted, ring B is an optionally substituted aryl group or an optionally substituted heteroaryl group, X1 is a group represented by -NR3-Y1-, -0-, -S-, -SO-, -SO2- or -CHR3- wherein R3 is a hydrogen atom or' an optionally substituted aliphatic hydrocarbon group, or R3 may be bonded to the carbon atom of ring B to form an optionally substituted ring structure, and Y1 is a bond or an optionally substituted C1-4 alkylene, R1 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, the formula = shows a single bond or a double bond, when ===R2 is - R2, R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, and when ===R2 is =R2, R2 is an oxo group, an optionally substituted alkylidene group, or an optionally, substituted imino group.
US20130023560 Methods and compositions for the treatment of iron toxicity Methods and compositions for the treatment of iron toxicity using nitroxides, particularly 4-hydroxy-2,2,6,6-tetramethyl-1-piperidine-1-oxyl (Tempol), N-acetylcysteine (NAC), and combinations thereof.
CA2335383C Protective coating for tablet A coated tablet and process for making the same is provided. A molten composition comprising at least 50 weight percent of a thermoplastic material having a melting point of less than about 120° C is applied to the tablet, and the molten composition is solidified into a protective coating. If desired, one or more outer coatings may be applied over the protective coating.
CN101028243A Anti-cancer composition containing neoformative vascular inhibitor and Eps mycin An anticancer composition containing neovascular inhibitor and epothilone and able to be made into slow-release implant or injection is composed of the slow-release microballs and solvent. Said slow-release microball consists of active anticancer component (neovascular inhibitor and/or epothilone) and slow-release additives (p (LAEG-EOP), p (DAPG-EOP), etc). Said solvent is an ordinary solvent or the special solvent containing the suspending aid.
EP2702999A1 Brain-targeting functional nucleic acid and use thereof The purpose of the invention is to provide a novel therapeutic agent for Alzheimer's disease and use thereof Provided is a therapeutic agent for Alzheimer's disease, which contains a CpG oligodeoxynucleotide structure having a brain migration and improved stability or a salt thereof as an active ingredient.
CN101313999A Pellet composition for promoting the reunion of fractured bones The invention relates to a method for manufacturing a composition of a muscle and ligament pill. The method comprises the following steps that: raw material medicines including rhubarb, raw eucommia barks, woodlouses, armadillo scales, pawpaw, radix sileris, achyranthes, raw radix aconiti feri, raw radix aconite, phrymaceae, dried fruit of citron or trifoliate orange, gentiana macrophylla, clematis chinensis, Chinese angelica, angelica dahurica, heracleum hemsleyanum michaux, coralbean barks, slender acanthopanax barks, safflower, asarum sieboldi, cimicifuga foetida, Chuanxiong rhizome, Japanese ampelopsis, notopterygium roots, radix stephaniae tetrandrae, Chinese atractylode rhizome and uncaria are ground together into fine powder; dragon blood and muskiness are added into the fine powder; and balsam and lead powder are used for decocting the fine powder into ointment. The composition has the main functions of dredging channels and collaterals, stimulating blood circulation to end stasis and reducing swelling and alleviating pain, and has the advantages that: the composition is quick to take effect and simple and convenient to use, and is economical and practical.
CN101423489A Indoline-2-one derivates and uses thereof The invention provides indoline-2-ketones derivatives, which have function of inhibiting propagation for multiple cancer cell strains, in particular have remarkable inhibiting effect on multiple cancer cell strains such as human leukemia K562 cells, human lung cancer A549 cells, human liver cancer HepG2 cells, and the like, and have wider anti-tumor spectrum. The derivatives have reasonable structural design, are screened out chemical entities of novel anti-tumor medicaments for providing a novel approach for rehabilitation of clinical tumor patients, can be applied to preparing anti-tumor medicament, and have wider anti-tumor spectrum.
USRE40901 14- Beta -hydroxy-1,14-carbonate-baccatine III and V derivatives, 13-substituted by an isoserine residue; remarkable cytotoxic and anticarcinogenic-agent activities; capable of overcoming the resistance of cell lines expressing the multidrug resistant phenotype; breast, ovarian, colon cancers A novel taxane derivative with anticancer activity, a process for its preparation and a process for the preparation of 14-β-hydroxy-1,14-carbonate-baccatine III and V derivatives 13-substituted by an isoserine residue.
US20050197383 Quaternary ammonium compounds and their use as anti-tussive agents In one aspect, the present invention concerns the use of certain quaternary ammonium compounds as active ingredient in the manufacture of a medicament for use in the treatment aid/or prevention of cough in warm-blooded animals, including humans, such as compounds of formula Y-J-EAn− (I), wherein J is independently selected from a group represented by one of formulae (II), (III) and (IV).
CN101513412A Application of 1,28-dyhydroxy-oleanane-2,12-diene in preparing medicament for treating skin diseases The invention discloses application of 1,28-dyhydroxy-oleanane-2,12-diene in preparing a medicament for treating skin diseases, and provides a pharmaceutical composition. The pharmaceutical composition is characterized by comprising the 1,28-dyhydroxy-oleanane-2,12-diene (I) which is taken as an active component and one or more medicinal accessories. In the pharmaceutical composition provided by the invention, the medicinal accessories are all administrative accessories which are suitable for the skin or mucosa.
WO2014032801A1 Fluoromethyl-substituted pyrrole carboxamides The invention relates to pyrrole carboxamides bearing a fluoromethyl- moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
US20100273725 Novel compounds useful in therapeutic and cosmetic methods The present invention relates to photosensitizer compounds for use in cosmetic and therapeutic applications of photodynamic therapy. The compounds of the present invention are designed for topical application and are characterized by a low permeability to the stratum corneum (the outer skin layer of an individual) and/or a low allergenic potential. Surprisingly, such compounds have beneficial properties in the treatment of certain diseases and lack the undesired damages to healthy skin entailed by prior art compounds. ALA (5-aminolevulinic acid)-esters of body-owned, natural compound such as aminoacids, steroids, carbohydrades, alcohols are preferred, examples of photosensitizers of the present invention. The compounds of the present invention are used in the treatment of skin diseases such as psoriasis, sebaceous glands related conditions including acne, seborrhoic dermatitis, rosacea, skin cancer and precancer, as well as in cosmetic hair removal.
CN1857273A Ursolate microballoon preparation and its preparing process The present invention discloses a kind of ursolic acid lipoid microballoon preparation, and each 1000ml of the ursolic acid lipoid microballoon preparation contains ursolic acid 0.2-50.0g, vegetable oil for injection 50-300g, emulsifier 5-20g, isoosmotic regulator 20-60g and water for injection for the rest. Its preparation process includes dissolving, heating, mixing, emulsifying, cooling, filling and other steps. The present invention overcomes the demerit of water insolubility of ursolic acid, and the ursolic acid lipoid microballoon preparation has less toxic reaction, less stimulation, long medicinal acting period and targeting property. The ursolic acid lipoid microballoon preparation has both disease treating effect and energy providing function.
WO2013067125A1 Co-activation of mtor and stat3 pathways to promote neuronal survival and regeneration Disclosed herein is a method of promoting sustained survival, sustained regeneration, in a lesioned mature neuron, sustained compensatory outgrowth in a neuron, or combinations thereof. The method comprises contacting the lesioned mature neuron with an effective amount of an inhibitor of PTEN and an effective amount of an inhibitor of SOCS3 to thereby promote survival and/or regeneration and/or compensatory outgrowth of the neuron. Therapeutic methods of treatment of a subject with a neuronal lesion by administration of a therapeutically effective amount of an inhibitor of PTEN and a therapeutically effective amount of an inhibitor of SOCS3, are also disclosed, as are pharmaceutical compositions and devices for use in the methods.
CN103006669A Application of tanshinone IIA to giving play to anti-tumor effect mechanism via FOXO1 pathway The invention relates to the field of natural drugs and in particular relates to a tanshinone IIA mediated anti-tumor mechanism via an FOXO1 dependence pathway. The invention discloses the effect of tanshinone IIA on inducing apoptosis of a non-small cell lung cancer cell strain A549 via the FOXO1 dependence pathway. In the non-small cell lung cancer cell strain A549, tanshinone IIA induces the FOXO1 mRNA level and protein level to rise in a time-dependent manner to promote an FOXO1 protein to be transported to a cell nucleus from cytoplasm. After an endogenous FOXO1 gene is silenced by FOXO1 siRNA, the cytotoxic effect, DNA damage effect and apoptosis inducing effect of tanshinone IIA are obviously reduced.
CA2187186C Stable aqueous folinate solution The invention provides an aqueous folinate solution suitable for medical applications in the form of a sodium folinate solution which is stable when stored at refrigerator temperatures, i.e. does not crystallize.
CN103142581A Application of natural compound luteolin in anti-hepatitis B virus The invention relates to an application of a natural compound luteolin in anti-hepatitis B virus, in particular provides an application of the compound luteolin in the preparation of anti-hepatitis B virus drugs, and specifically provides an application of the compound in the preparation of drugs which inhibit expression of hepatitis B virus HBsAg and HbeAg; aiming at the problem that the existing anti-hepatitis B virus drugs have a relatively high toxicity, the cell toxicity of HepG2.2.15 cells with anti-hepatitis B virus in vitro and the inhibiting effect on excretion of HBsAg and HBeAg are detected, the results show that the compound luteolin has a relatively low toxicity to HepG2.2.15 cells and has a relatively high inhibiting activity to HBsAg and HBeAg. The compound luteolin provided by the invention is widely spread in nature, and therefore the raw material source is wide and abundant.
CN103127017A Entecavir dispersible tablet and preparation method The invention discloses an entecavir dispersible tablet and a preparation method, the entecavir dispersible tablet is characterized in that entecavir and a solid dispersion carrier are solved in an absolute ethyl alcohol, then a disintegrating agent which is insoluble in water is uniformly dispersed, dried under reduced pressure to remove absolute ethyl alcohol to obtain the solid dispersion attached on the surface of the disintegrating agent, and then the tablet is directly compressed with the pharmaceutically acceptable auxiliary materials. The entecavir dispersible tablet can avoid the problem of difficult removal of solid dispersion due to certain viscosity, the dissolution rate of the product can be greatly increased, the preparation method is simple, the operation is convenient, and the entecavir dispersible tablet is suitable for industrialized mass production.
US20120208809 9h-pyrrolo[2,3-b: 5,4-c'] dipyridine azacarboline derivatives, preparation thereof, and therapeutic use thereof The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c′]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers and salts of said substances of formula (I) and to the therapeutic use thereof for treating cancer.
WO2006108965A3 Npy antagonists, preparation and use The invention relates to novel compounds, to the preparation and use thereof, in particular therapeutic. Said invention particularly relates to derived compounds comprising at least two aromatic cycles, to the preparation and use thereof, mainly for human and animal health care. Said compounds exhibit an affinity to biological receptors Y and NPY of a neuropeptide Y which are present in the central and peripheral nervous systems. The inventive compounds are preferably embodied in the form NPY antagonists, and more particularly in the form of NPY Y1 subtype antagonists and, whereby are usable in therapeutic or prophylactic treatment all NPY involving disorders. Pharmaceutical compositions comprising said compounds, the preparation and the use thereof and treating methods using said compounds are also disclosed.
US20090062378 Nutraceutical Mangosteen Composition Nutraceutical compositions derived from the fruit of the Garcinia mangostana L. or mangosteen plant and methods to make the same are provided. The nutraceutical mangosteen compositions employ novel combinations of mangosteen fruit pulp and pericarp, and can be additionally complemented by selected juice concentrates to yield a composition for improving general health and wellness in humans. The methods to make the nutraceutical compositions involve the use of a mixture comprising pericarp and inner pulp from whoe fruit of a Garcinia mangostana L. plant.
CN1872134A Composition of bitter melon polysaccharide for reducing blood sugar, and preparation method A hypoglycemic momordic polyose composition suitable for the diabetics is prepared from balsam pear through refluxing in organic solvent, extracting by water or alkali, and depositing in alcohol.
CN101703448A Direct compression process for cefuroxime axetil dispersible tablets The invention relates to a direct compression process for cefuroxime axetil dispersible tablets, which is characterized in that: the following raw materials and auxiliary materials are sieved through a 40 mesh sieve and are mixed for thirty minutes in a mixing tank, and then the mixed powder materials are directly compressed by a high speed rotary tablet press to form the cefuroxime axetil dispersible tablets; and based on 125 grams of cefuroxime axetil, the raw materials and the auxiliary materials for producing 1000 dispersible tablets comprise 25 grams of cefuroxime axetil, 4 to 10 grams of stearic acid, 210 to 250 grams of microcrystalline cellulose, 28 to 35 grams of croscarmellose sodium, 2 to 4 grams of silicon dioxide and 2 to 4 grams of sodium dodecyl sulfate. The direct compression process for the cefuroxime axetil dispersible tablets improves the dissolution rate of the cefuroxime axetil dispersible tablets and improves the bioavailability and the healing effect of the medicament, wherein the dissolution rate reaches 99.5 percent at the time when the tablets dissolve for 45 minutes. The direct compression process simplifies the production process, shortens the production period and saves energy.
CN101229139A Cefathiamidine freeze-dried powder injection and preparing method thereof The invention which discloses a preparation method of cephathiamidine freeze-dried powder injection is characterized in that the cephathiamidine is dissolved in the temperature of 40 to 60 DEG C and after the color removal through activated carbon and filtration, the hot solution is rapidly cooled to minus 41 to minus 30 DEG C in a freeze drier; the temperature is reduced to minus 60 to minus 50 DEG C and the vacuum is pumped and the temperature rises to 20 to 30 DEG C gradually; the obtained cephathiamidine freeze-dried powder injection has the average yield of more than 98 percent, water content of less than 0.4 percent, stable quality of drugs, uniform crystallization and color and plump appearances.
EP2223926A1 Pyridine derivative substituted with heterocycle and phosphonoxymethyl group and antifungal agent containing the same The present invention provides antifungal agents that have excellent antifungal action, and is also excellent in terms of its properties, particularly its solubility in water and its safety. According to the present invention, disclosed are compounds represented by the following formula (I): (wherein R1 represents a hydrogen atom, a halogen atom, an amino group, R11-NH-(wherein R11 represents a C1-6 alkyl group, a hydroxy C1-6 alkyl group, a C1-6 alkoxy C1-6 alkyl group, or a C1-6 alkoxycarbonyl C1-6 alkyl group), R12-(CO)-NH- (wherein R12 represents a C1-6 alkyl group or a C1-6 alkoxy C1-6 alkyl group), a C1-6 alkyl group, a hydroxy C1-6 alkyl group, a cyano C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group, or a di-C1-6 alkylamino group; one of X and Y represents a nitrogen atom, and the other represents a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, -CH2O- -OCH2-, -NH-, -CH2NH-, -NHCH2-, -CH2S-, or -SCH2-; R3 represents a hydrogen atom or a halogen atom, or a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or a 5- or 6-member non-aromatic heterocyclic group, wherein these groups may have one or two substituents selected from a substituent group α; and R4 represents a hydrogen atom or a halogen atom; [substituent Group α] a halogen atom, a cyano group, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkoxycarbonyl group, a C3-8 cycloalkyl group, a C2-6 alkenyl group, and a C2-6 alkynyl group).
EP1699464A1 Menstrual cycle control and improvement of conception rates in females The present invention relates to methods of increasing likelihood of conception, treatment of low fecundity and/or providing menstrual cycle control without suppressing ovulation in a female comprising administering an effective dose of at least one estrogen and at least one progestin within a treatment period of at least 21 days to 35 days or multiple periods thereof. Furthermore, the invention relates to the combination of at least one estrogen and at least one progestin for the preparation of a medicament to be used in the abovementioned indications. A pharmaceutical kit, according to the invention, comprises 21 to 35 dosage units or a multiple of 21 to 35 dosage units, wherein - a first section comprises at most 21 dosage units of at least one estrogen; and - a second section comprises from 2 to 34 dosage units of at least one estrogen and from 2 to 34 dosage units of at least one progestin or comprises from 2 to 34 dosage units of at least one estrogen and at least one progestin provided that in each dosage unit containing a progestin or a progestin and an estrogen the progestin is in a nonovulation inhibiting amount; and ; and - optionally a third section comprises at most 10 dosages of a pharmaceutically acceptable placebo or a blank.
US7291617 Arylamidine derivative or salt thereof An arylamidine derivative represented by a general formula described below or a salt thereof has an excellent antifungal action and high safety, and it is useful as an antifungal agent with good pharmacokinetics and pharmacodynamic properties wherein X represents an unsubstituted or substituted lower alkylene or alkenylene group; G1 represents an oxygen atom, a sulfur atom, or an imino group; G2 represents a carbon atom or a nitrogen atom; Ra represents at least one group selected from the group consisting of a hydrogen atom, a halogen atom, and unsubstituted or substituted alkyl, cycloalkyl and alkoxy groups; R1 represents an unprotected or protected or unsubstituted or substituted amidino group; and R2 represents a substituted amino or substituted cyclic amino group, or the like.
US20110130352 The use of the effective fraction of alkaloids from mulberry twig in preparing hypoglycemic agents The present invention relates to an effective fraction of alkaloids and the effective fraction is prepared from mulberry twig and its active ingredients are a composition of alkaloids. Determined by HPLC, the percentage of the total alkaloids are 50% or more by weight in the effective fraction and the percentage of the compound 1-deoxynojirimycin is 30% or more by weight in the total alkaloids. The effective fraction of the invention is prepared as the following steps: the mulberry twig is extracted by solvents, and the extract is precipitated by alcohol precipitation or flocculation to remove the impurities, and then concentrated, purified by resin chromatography. The present invention also relates to a pharmaceutical composition containing the said effective fraction of alkaloids and to the use of the effective fraction of alkaloids according to claim 1-4 in preparing hypoglycemic agents.
WO2011065541A1 Anti-tumor effect potentiator An anti-tumor effect potentiator comprising, as an active ingredient, a uracil compound represented by formula (I) (wherein X represents a C1-5 alkylene group, wherein at least one of methylelen groups that constitute the alkylene group may be substituted by an oxygen atom; R1 represents a hydrogen atom or a C1-6 alkyl group; R2 represents a hydrogen atom or a halogen atom; and R3 represents a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl)-(C1-6 alkyl) group, a halogeno-(C1-6 alkyl) group or a saturated heterocyclic group) or a pharmaceutically acceptable salt thereof.
CN101037419A Crystalline parecoxib sodium A process for producing crystalline form I of cabergoline, which process comprises the preparation of Form V using heptane as precipitation solvent, and its exclusive conversion into crystalline Form I of cabergoline. The present crystallization process from toluene-heptane solvent system for form V involves ''reverse addition'' of toluene-cabergoline concentrate to cold heptane.
CN103374012A Salt of sanguinarine derivative The invention relates to fumarate of sanguinarine and a derivative, or pharmaceutically acceptable solvate thereof and an application of fumarate in preparation of a medicine used for treating hepatitis B.
US20050042653 Human transport protein homologs The invention provides a human transport protein homologs (HTPH) and polynucleotides which identify and encode HTPH. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating or preventing disorders associated with expression of HTPH.
EP1251847B1 Novel use of prodigiosin for treating diabetes mellitus The present invention relates to a novel use of prodigiosin for treating diabetes mellitus. The prodigiosin can treat or prevent diabetes mellitus without any side effect.
US20090035373 Pharmaceutical composition for contraception and blood pressure regulation, kit for contraception containing same and method of production of same The pharmaceutical composition for contraception and regulating blood pressure includes daily dosage units, which contain 2.0 mg of dienogest and 0.030 mg of ethinyl estradiol, 2.0 mg of dienogest and 0.020 mg of ethinyl estradiol, or 1.5 mg of dienogest and 0.015 mg of ethinyl estradiol, together with at least one excipient and/or carrier. Each daily dosage unit may be a coated tablet for oral administration consisting of a tablet core and a coating around the core. The coating contains all of the ethinyl estradiol and a part of the dienogest, which are released in a non-retarded fashion. The tablet core contains another part of the dienogest that is released in a retarded fashion. The risk of folate deficiency-induced congenital malformations in the event of pregnancy may be reduced by including (6S)-5-methyltetrahydrofolate in each daily dosage unit. A kit for a 28-day cycle is also disclosed.
US20110023137 Fusion protein comprising a caspase domain and a nuclear hormone receptor binding domain and methods and uses thereof The present invention relates to a fusion protein comprising a Caspase domain or a functionally active variant thereof and a ligand binding domain of a nuclear hormone receptor, a nucleic acid coding for the fusion protein, a vector or cell comprising the nucleic acid, a method of producing the fusion protein, a non-human transgenic animal containing the nucleic acid, the use of the fusion protein for ligand-mediated induction of apoptosis of a cell, or for studying the function of a cell, tissue and/or organ or the use of a transgenic organism for studying the function of a cell at various developmental stages or as a disease model, a method for inducing apoptosis of a cell expressing a fusion protein or for identifying a ligand, or a medicament comprising a fusion protein, the nucleic acid, the vector or the cell, particularly for the treatment of cancer or for or after transplantation, particularly as safety mechanism.
US20120196863 1,4 oxazines as bace1 and/or bace2 inhibitors The present invention provides 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
EP1370228B1 Systems for delivering a cosmetic and/or therapeutic active to oral surfaces Systems for delivering cosmetic and therapeutic actives to the oral cavity employ a strip comprising a first layer of material, a second layer comprising polybutene with a molecular weight of about 300 to about 3000, and a cosmetic or therapeutic active included within the second layer. Therapeutic and cosmetic actives in compositions comprising polybutene inhibit or prevent gingivitis, caries, staining, fungi, bacteria and plaque build-up in the oral cavity by means of the delivery system.
CN102652733A Natural progesterone proliposome preparation and preparation method and using method thereof The invention discloses a natural progesterone proliposome preparation and a preparation method and a using method thereof. The natural progesterone proliposome preparation contains 1 to 30 percent of progesterone in percentage by weight, and is prepared from progesterone, phosphatide, 1,2-propanediol or/and poly(ethylene glycol)-400 (PEG-400). The natural progesterone proliposome preparation is diluted with water before being taken, or is orally taken into a body, and contacts body fluid, and the phosphatide is hydrated and self-assembled to form liposome. The natural progesterone proliposome preparation avoids metabolizing of progesterone in gastrointestinal tracts and reduces the first pass effect by using a wrapping function of the liposome, and cellular barriers can be changed by using the liposome so as to promote transmembrane transport and inhibit P-glycoprotein to realize slow releasing; and the natural progesterone proliposome preparation has the functions of good cytocompatibility, promotion of lymphatic transport and the like so as to promote gastrointestinal absorption of natural progesterone. Meanwhile, the natural progesterone proliposome preparation can be further modified by chitosan which promotes absorption and has strong adhesivity to further improve the bioavailability of the progesterone. Therefore, the natural progesterone proliposome preparation is a novel preparation which improves the absorption and the bioavailability of the progesterone after oral administration from a variety of mechanism and a plurality of angles.
WO2013160728A1 Dual targeting compounds for the treatment of alzheimer's disease Compounds of formula (I) wherein the groups are as defined in the description, are used as medicaments, in particular for the treatment of a disease selected from the group consisting of: cognitive impairment, memory dysfunction, neurodegenerative disorders and related dementia, Alzheimer's disease, Parkinson's disease, neuropsychiatric behavior associated with Alzheimer's disease, pain, depression, attention deficit hyperactivity disorder and for pharmacological addictive substance or intoxicant therapy; and for the neuroprotection from NMDA toxicity.
CN102161647A Preparation method and applications of isoflavone type multidrug resistance reversal agent of cancer cell The invention relates to the pharmaceutical chemistry field, in particular to isoflavone type compounds (I), a preparation method of the compounds, medicinal composites with the compounds and medicinal applications of the compounds and the medicinal composites, in particular to the applications used as the multidrug resistance reversal agent of cancer cell.
WO2010121570A1 Methyl cantharimide compounds, treatment method using them and their preparation method Methyl cantharimide compounds, the treatment method using them and their preparation method are disclosed. The methyl cantharimide compounds contain the main chain as shown by the following formula (I): wherein R1, R2, R3 and R4 are respectively selected from H, C(O)OR5, C(O)R6, C(O)NR7R8, NR9C(O) R10, N-R11R12, O-R13, S-R14, P(O) (OR15) (OR16), As(O) (OR17) (OR18), SO2R19, SO3R20 and B(OR21); X1-X4 are respectively selected from nitrogen or carbon; R1-R4 are not all hydrogen; Y1, Y2 and R5-R21 are respectively selected from hydrogen, C1-12 alkyl, aryl, heterocyclic group and a bioactive polymer. The methyl cantharimide compounds of the invention have lower cytotoxicity to normal cells and have higher cytotoxicity to cancer cells.
WO2009140201A1 Methods for preventing the development of retinopathy by the oral administration of nnr ligands Method and compositions for delaying the onset or progression of retinopathy, including administering at least one neuronal nicotinic ligand are disclosed.
WO2010015324A1 Quinuclidine carbonate derivatives and medicinal composition thereof The invention relates to quinuclidine carbonate derivatives acting as muscarinic receptor antagonists, to methods of preparing such derivatives, to compositions comprising them and therapeutic use thereof.
US20050064037 Transdermal delivery of oxybutynin in gel formulations A topical gel formulation of oxybutynin is provided that exhibits enhanced bioavailability, minimized adverse side effects and skin irritations, and improved patient compliance compared to the existing oral and transdermal formulations of oxybutynin.
EP1773770A1 Indole-2-carboxamidine derivatives as nmda receptor antagonists The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I) - wherein the meaning of X is hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C1-C4 alkyl, C1-C4 alkoxy group, or the neighboring V and Z groups in given case together with one or more identical or different additional hetero atom and -CH= and/or -CH2- groups can form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably benzene, dioxolane ring, A, B and C independently are substituted carbon atom or one of them is nitrogen atom, and the salts thereof. Further objects of the invention are the processes for producing indole-2-carboxamidine derivatives of formula (I), and the pharmaceutical manufacture of medicaments containing these compounds, as well as the process of treatments with these compounds, which means administering to a mammal to be treated - including human - effective amount/amounts of indole-2-carboxamidine derivatives of formula (I) of the present invention as such or as medicament. The new indole-2-carboxamidine derivatives of formula (I) of the present invention are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.
CN101278914A Cefpodoxime proxetil suspension composition and preparation thereof The invention relates to a cefpodoxime proxetil dry suspension composition and a preparation method thereof. The invention provides the cefpodoxime proxetil dry suspension composition, containing 100 parts by weight of the cefpodoxime proxetil and 20 to 500 parts by weight of the glyceryl behenate. The invention also provides the preparation method of the dry suspension composition. The dry suspension composition of the invention is capable of reducing bitterness of the cefpodoxime proxetil remarkably and improving compliance of a clinical patient, thereby being suitable for a child to take a drug.
WO2007050643A3 Compositions and their uses for gene therapy of bone conditions The present invention provides compositions for the treatment of conditions associated with low' bone density. The compositions comprise a payload molecule that comprises a nucleic acid selected from the group consisting of an oligonucleotide, an antisense construct, a siRNA, an enzymatic RNA, a mRNA, a recombinant DNA construct, a linear DNA fragment, a blocked linear DNA fragment and a mixture thereof ; a payload trapping molecule selected from the group consisting of chitosan, polyehtylenimine, poly-L-lysine, alginate, xanthan, hexadecyltrimenthylammoniumbromide and mixtures thereof ; and a carrier selected from a yeast particle or a yeast glucanmannan particle.
US20050130221 Synthesis for the preparation of compounds for screening as potential tubulin binding agents The present invention relates to methods for the synthesis of chemical compounds for screening as potential tubulin polymerization inhibitors. The invention also provides chemical compounds with tubulin polymerization inhibitor activity.
CN102131811A Oxazolidinone derivative having fused ring Disclosed is a novel anti-bacterial agent comprising a compound represented by formula (I), a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt. In formula (I), the ring A is a group represented by formula (A-1), (A-2), (A-3) or (A-4); the ring B represents an optionally substituted benzene ring; the ring C represents an optionally substituted 6-membered hetero ring which contains at least one N atom, contains C as an atom to which the ring B is bound, and has 1 to 3 double bonds in the ring; the ring D represents an optionally substituted 5-membered ring having 1 to 2 double bonds in the ring; A1 and A2 independently represent N or C; m represents a number of 0 or 1; R represents H, -NHC(=O)RA, -NHC(=S)RA, -NH-het1, -O-het1, -S-het1, -S(=O)-het1, -S(=O)2-het1, het2, -CONHRA, -OH, a lower alkyl, a lower alkoxy, or a lower alkenyl; and het1 and het2 independently represent a heterocyclic group.
CN102652835A Sustained-release polymer retinoic acid Retinoic acids [all-trans retinoic acid and artificially synthesized retinoic acid] are derivatives of vitamin A. These vitamin A derivatives have important effect on the growth, differentiation, and maintenance of epithelial cells. The sustained-release polymer retinoic acid of the invention is soluble in water, and the pharmaceutically biological activity is assessed. In vitro, both retinoic acid and sustained-release polymer retinoic acid can inhibit the differentiation of tumor cells and induce tumor cell apoptosis, and targeted combination of the polymer with 'bad phagocytes' which swallow tumor substances is helpful for the combination of retinoic acid with tumor cells; in vivo, the sustained-release polymer retinoic acid can inhibit tumor cell growth, and the effect is 6-8 times stronger than that of retinoic acid. The sustained-release polymer retinoic acid can enhance the anti-tumor curative effect of retinoic acid drugs and prolong drug action time, and thus can be effectively used for human tumor prevention and treatment.
US20130017247 Treatment and/or prevention of oral allergic symptoms caused by oral contact with fruits and/or vegetables Treatment or prevention of oral allergy syndrome, or other allergy-related oral inflammatory processes using a topical preparation of at least one of a mast cell stabilizer and an antihistamine is disclosed. For example, the topical administration of Cromolyn Sodium prior to ingestion of raw fruits and raw vegetables may be used to prevent oral allergy symptoms. The topical administration can be performed by use of a solution, a powder, an aerosol, a tablet, a chewable tablet, a gel, a melting strip, a mouth rinse, a mouth swab, or a piece of candy, and may be combined with carrier molecules and/or mucoadhesive molecules to enhance efficacy.
US20100144686 Topically applicable anti-inflammatory o/w emulsions comprising pro-penetrating glycols Stable, topically applicable, non-greasy and non-tacky oil-in-water (O/W) anti-inflammatory emulsions, useful, e.g., for the treatment of psoriasis, contain: a. a therapeutically effective amount of at least one steroidal anti-inflammatory agent, notably clobetasol propionate; b. a pro-penetrating system which includes at least one pro-penetrating glycol and at least one other pro-penetrating agent; and c. at least one polymeric emulsifier not sensitive to electrolytes, for example not an acrylate/C10-C30 alkyl acrylate copolymer, formulated into a topically applicable, pharmaceutically acceptable vehicle therefor.
CN101045057A Application of tetramethylpyrazine for preparing medicine to treat neovascular retina diseases An application of ligustrazine in preparing the medicines for treating the neovascular retinopathy is disclosed.
US20080269252 Use of Compounds Derived From Pyrimidinetrione as Acetyl Cholinesterase Inhibitors, Compositions Containing Said Derivatives, and the Uses Thereof The invention relates to the use of compounds derived from pyrimidinetrione of general formula (I) as acetyl cholinesterase (AChE) inhibitors. The invention also relates to the use of said compounds as insecticides, and to compositions containing the same.
WO2006028122A1 Agent for preventing and ameliorating obesity An agent for preventing and ameliorating obesity; and a material for foods, drugs and so on which can exert effects of preventing and ameliorating the onset of various life style-related diseases such as preventing and ameliorating hyperlipemia, has a high safety, is applicable over a wide range and scarcely worsens food texture. Namely, an agent for preventing and ameliorating obesity comprising, as the active ingredient, acetylated starch or octenyl succinic acid-modified starch; an agent for preventing and ameliorating obesity; an inhibitor for visceral fat accumulation; an inhibitor for blood glucose level elevation; or an agent for preventing and ameliorating diabetes.
WO2012098066A1 1,6- and 1,8-naphthyridines useful as dyrk1 inhibitors Compounds of formula I, and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
US6921824 Ruthenium dimeric complexes suitable as antimetastatic and antineoplastic agents New ruthenium dimeric complexes with high antimetastatic and antitumour activity and remarkable chemical stability are described.
EP1202736B1 Nicotine in therapeutic angiogenesis and vasculogenesis The present invention features methods for induction of angiogenesis by administration of nicotine or other nicotine receptor agonist. Induction of angiogenesis by the methods of the invention can be used in therapeutic angiogenesis in, for example, treatment of ischemic syndromes such as coronary or peripheral arterial disease. The Figure is a graph illustrating the effect of intramuscularly administered nicotine upon capillary density in an animal model of ischemia.
US20100069345 Lanthanide-porphyrin complexes as anti-tumor agents The present invention relates to lanthanide porphyrin complexes and their uses as anti-tumor agents. The described complexes show promising cytotoxic properties toward cancer cells in both in vitro and in vivo studies.
CN102846633A Inhalant containing N-acetyl-L-cysteine and ciclesonide and preparation method thereof The invention relates to an inhalant containing N-acetyl-L-cysteine and ciclesonide and preparation method thereof. The inhalant is composed of ciclesonide and N-acetyl-L-cysteine as the active ingredients, and one or more pharmaceutical adjuvants suitable for inhalation drug delivery.
CN103690549A Preparation of alpha-hederin solid dispersion and its cyclodextrin inclusion compound The invention relates to preparation of a Fructus Akebiae alpha-hederin solid dispersion and an alpha-hederin cyclodextrin inclusion compound. In the solid dispersion, the alpha-hederin and a solid dispersion carrier are in a weight ratio of 1:1-1:200; and in the cyclodextrin inclusion compound, the alpha-hederin and cyclodextrin are in a mole ratio of 1:1-1:20. After preparation of the solid dispersion and the inclusion compound, the solubility, dissolution rate and bioavailability of alpha-hederin can be significantly improved.
WO2014011083A3 Pharmaceutical composition having improved flowability, medicinal agent, and method for producing and using same The invention relates to the field of pharmaceuticals, specifically to solid pharmaceutical compositions containing 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or a pharmaceutically acceptable salt thereof, a stabiliser, a lubricant and a filler, and also to methods for producing said pharmaceutical composition and to medicinal agents for suppressing the immune system and treating multiple sclerosis. 2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol is an immunomodulator which causes a redistribution of lymphocytes from the blood flow to the secondary lymphatic tissue, thus leading to immunosuppression. The invention provides a uniform distribution of the active component in a solid composition, high stability and the improved flowability of a solid pharmaceutical composition. This improved flowability allows for the use of the compositions proposed in the invention in conjunction with automatic equipment.
US7550480 1,8-naphthyridin-2(1H)-ones; treating CSBP/p38 kinase mediated diseases; cytokine suppressive anti-inflammatory drugs Novel substituted 1,5,7-trisubstituted-1,8-napthyridin-2(1H)-one compounds; 1,5,7 trisubstituted-1,6-napthyridine-2-(1H)-one compounds and 1,5,7-trisubstituted quinoline-2(1H)-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.
WO2012000253A1 Composition for injection comprising docetaxel and preparation method thereof A composition for injection comprising docetaxel and polysorbate 80, wherein the mass ratio between docetaxel and polysorbate 80 is 1 : 26.75. The preparation method of the composition is as follows: 1) formulating the stock solution by adding polysorbate 80 to a tank and then adding absolute ethanol slowly with stirring until the density of the stock solution being 0.886~0.896g/ml; 2) dissolving docetaxel in the stock solution; 3) the resulted solution being filtered and distributed in sterile condition and then vacuum drying to remove the ethanol.
WO2013020245A1 Carbonyl derivatives of betulin Disclosed are a compound characterized by the following formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising said compound or a pharmaceutically acceptable salt thereof, wherein R3, L, and A are as described in the application. Said compounds are useful for the treatment of HIV.
WO2008121064A1 New imidazo[4,5-b]pyridine-6-halo-7-aryl/heteroaryl compounds 705 The present invention relates to new compounds of formula (I) as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
US7256178 Physiologically active substances Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R3, R7, R16, R17, R20, R21 and R21′ are the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.
CN101062117A Capsule for eliminating phlegm and relaxing heart Disclosed is an oral liquid for treating thyroid tumor, nodular goiter, psoriasis, epoophoron cyst and eczema, which is prepared from dyer's woad, frankincense, myrrh, black catechu, natural indigo, orpiment, Bupleurum root, and bee glue through steps of proportioning, washing, disintegrating, sieving and loading into capsules.
EP2211869A2 Idarubicin for the treatment of lymphoma in a dog The present invention relates to a method of treating a lymphoma in a dog comprising administering to a dog in need of such treatment a therapeutically effective amount of idarubicin or a pharmaceutically acceptable salt thereof.
CN103122298A Magnet healthcare medicated wine The invention discloses a magnet healthcare medicated wine, and relates to a healthcare functional medicated wine utilizing a magnet and having the function of alleviating tinnitus. The invention aims at providing a healthcare functional medicated wine utilizing a magnet and having the function of alleviating tinnitus, wherein the medicated wine has the functions of alleviating tinnitus symptoms, tonifying liver and nourishing essence, strengthening the spleen and stomach, and prolonging life. The aim of the invention is realized via the following technical scheme: the magnet healthcare medicated wine comprises the following constituents: 300 g of magnets, 50 g of dogwood, 50 g of saposhnikovia divaricata, 40 g of Chinese yam, 50 g of acorus calamus, 60 g of polygala tenuifolia, and 30 g of radix aconiti preparata, wherein the magnet healthcare medicated wine is obtained by placing the constituents aforementioned in wine and soaking for one month, and the weight of the wine is 5000 g. In the scheme, the constituents further comprise 30 g of fructus viticis, 20 g of chrysanthemum, 20 g of ligusticum wallichii, 40 g of asarum, and 50 g of cinnamon. In the scheme, the constituents further comprise 10 g of rhizoma zingiberis, 20 g of poria cocos, and 80 g of radix rehmanniae preparata.
EP2055308A1 Pharmaceutical for promoting functional regeneration of damaged tissue The present inventors revealed the following for the first time in the world: 1) a large amount of bone marrow-derived cells are mobilized to grafted skin; 2) the mobilized bone marrow-derived cells are differentiated into any of dermal fibroblasts, adipocytes, muscle cells, vascular endothelial cells, and epidermal keratinocytes in the grafted skin, and the mobilized bone marrow-derived cells include bone marrow-derived mesenchymal stem cells; 3) the factors which mobilize bone marrow-derived mesenchymal stem cells from peripheral blood to the grafted skin are HMGB1, HMGB2, and HMGB3 released from the necrosed tissue of recipient skin; 4) purified HMGB1, HMGB2, and HMGB3 promote the migration of mesenchymal stem cells isolated and cultured from bone marrow; 5) activators containing HMGB1 which allows the migration of bone marrow mesenchymal stem cells can be conveniently purified from several organ extracts including skin, brain, and heart; 6) activators which allow the migration of bone marrow mesenchymal stem cells can be conveniently extracted from cultured cells; and 7) a heparin-column purified fraction of skin extract mobilizes a large amount of bone marrow-derived cells in case of brain injury.
CN1723908A Gelatin micro-particles carried with dichloromethylene diphosphonate, and its prepn. method A gelatin micro-particle carrying dichloromethylene diphosphonic acid for treating immune thrombocytopenic purpura ( ITP ) ,AIDS and typhoid is prepared through treating gelatin to make its granularity be 200-7nm and positively charged, and linking dichloromethylene diphosphonic acid. Its advantages are high curative effect, biodegradability and biocompatibility, and low poison.
CN1660062A Lysine acetic acid in use for injection A freeze-dried powder injection of lysine acetate for intravenous drip is prepared from lysine acetate through aseptic dissolving and freeze drying.
US20050215637 Tuberculosis treatment A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.
CN103127114A Medicinal composition including piperacillin sodium and sulbactam sodium The invention belongs to the technical field of medicaments, and in particular relates to a medicinal composition including piperacillin sodium and sulbactam sodium. The medicinal composition is an injection, and an X-ray powder diffraction spectrogram, which is obtained through Cu-K alpha-ray measurement, of a sulbactam sodium compound in the medicinal composition is as shown in figure 1. The sulbactam sodium has very good storage stability, and the medicinal composition including the piperacillin sodium and the sulbactam sodium has better storage stability and high use safety; moreover, the medicinal composition including the piperacillin sodium and the sulbactam sodium has better accumulating, synergistic and complementary functions, and is better in bioavailability.
CN101508713A Glucoside containing 1,2,3-triazole structure, preparation method and application The invention relates to the diabetes-related drug field. More specifically, the invention relates to an sodium glucose transporter 2 (SGLT2) inhibitor containing a 1,2,3-triazolylglucoside structure, a preparation method and application thereof to preparation of antidiabetic drugs, wherein, radicals are defined as in the specification.
WO2011047596A1 Use of hydroxy benzopyrone compounds for preparing medicine useful for for precaution and treatment of fracture and osteoporosis Disclosed is a use of compound of formula(Ⅰ), pharmaceutically acceptable salts or pharmaceutical composition thereof for preparing a medicine for the precaution and the treatment of fracture, osteoporosis and the disorders regulated by female hormone receptor subtypes of ER-α and ER-β.
US20090227556 Receptor tyrosine kinase inhibitors comprising pyridine and pyrimidine derivatives A compound represented by the following formula, a salt thereof or a hydrate of the foregoing can inhibit VEGFR-1, VEGFR-2, VEGFR-3, RON, RET and/or KIT. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH═, nitrogen or the like.]
USRE39149 Method of administering azithromycin An oral dosage form of azithromycin which does not exhibit an adverse food effect; Specific azithromycin oral dosage forms including tablets, powders for oral suspensions and unit dose packets; Methods of treating microbial infections with the dosage forms; And therapeutic packages containing the dosage forms.
CN102552218A Memantine hydrochloride capsule sustained-release preparation and preparation method for same The invention discloses a memantine hydrochloride capsule sustained-release preparation, wherein the preparation is composed of two parts, namely, immediate-release grains and sustained-release grains; the sustained-release part is composed of a blank pellet core, a medicine layer and a release control layer; and the immediate-release part is composed of a blank pellet core and a medicine layer. The capsule is uniform in content, good in release effect, stable in blood concentration, good for reducing the toxic and side effects of medicines, and is capable of being used for treating moderate-to-severe Alzheimer-type dementia, and the medicine-taking times of the patient are reduced,.
CN101204382A Mitomycin double sustained release film of implanted antineoplastic agents and its preparation method The invention discloses a double controlled release film agent of implanted antineoplastic agent mitomycin and a manufacturing method; the invention relates to a medicinal controlled release film agent. The invention provides a double controlled release film agent of implanted antineoplastic agent mitomycin, which relates to a medicinal controlled release film agent with high enveloping ratio, long continuous release duration, small incidence of burst release, few toxic and side effects, high medicine concentration on tumor lesions and low recrudescence probability of tumor, and a manufacturing method. The film agent includes mitomycin, polymer, lecithin, chitosan and collagen. The mitomycin and the lecithin are dissolved, lyophilized in order to obtain a colloidal mixture; the polymer is dissolved in organic solvent in order to obtain a polymer solution; the polymer solution is then added in the colloidal mixture in order to obtain a reverse micelle; the reverse micelle is further added to a polyvinyl alcohol solution, and an O/W latex is obtained by emulsification; the latex is lyophilized in order to obtain carrier micro-spheres; the collagen is dissolved in the acid solution in order to obtain a collagen solution; the chitosan is dissolved in the acid solution in order to obtain a chitosan solution; the collagen solution and the chitosan solution are mixed in order to obtain a collagen-chitosan mixture solution; finally the carrier micro-spheres are dispersed in the collagen-chitosan mixture solution which is then poured in a mould and dried.
CN101979088A Medicament for treating cauma and empyrosis The invention relates to a medicament for treating cauma and empyrosis, which comprises 40 grams of Chinese angelica, 20 grams of astragalus, 30 grams of honeysuckle flower, 30 grams of wild chrysanthemum, 15 grams of mint, 20 grams of figwort root, 30 grams of mongolian dandelion herb, 180 grams of white sugar, 180 grams of high protein fat and 1,500 grams of rain water. The accuracy of the dose of the medicament is +/-10 percent. The medicament for treating the cauma and the empyrosis is mainly used for treating the cauma and the empyrosis such as flame burn, empyrosis by high-temperature objects, chemical cauma and empyrosis and the like, has short cure time and obvious curative effect, activates regeneration cells of subcutaneous soft tissue epidermis, can remove scars, is safe and does not have any toxic or side effect.
WO2008050207A1 Heterocyclic compounds useful as anabolic agents for livestock animals Compounds of formula (I) and pharmaceutically acceptable salts thereof are agonists at the beta-2 adrenoceptor. They are useful as feed additives for. livestock animals.
CN102802644A Mixtures of acids for use as antiviral agents The present invention provides mixtures of acids containing lactic acid, formic acid, tartaric acid, malic acid, citric acid and orthophosphoric acid for use in prophylaxis and/or treatment of viral diseases, particularly the foot and mouth disease in animals.
CN101711764B Tegafur compound capsules floating in stomach for curing gastric cancer The invention relates to a Tegafur compound capsule floating in the stomach for curing gastric cancer, wherein active medicine Tegafur, Jimeisita and Potassium Oxonate are evenly mixed with auxiliary materials, pelletizing is carried out through a dry method or a wet method, and finally capsules are filled. Tegafur compound preparation can be prepared into capsules floating in the stomach, which can target stomach, retain in the stomach for a longer time, slowly release medicine, improve the efficacy of Tegafur to gastric cancer, lower the peak value change of the medicine blood concentration, lower toxic and side effects of medicines and prolong the action time of medicines.
CN103027437A Health care shoe-pad The invention provides a health care shoe-pad. According to the health care shoe-pad, peppermint has the functions of dispelling wind and heat, clearing and disinhibiting head and eyes, being light and disperse, and relieving sore throat and promoting eruption; white alum has the functions of detoxification and killing insect and eliminating dampness and relieving itching, and therefore effects of eliminating peculiar smell, relieving itching and killing insect, and eliminating dampness and detoxification can be achieved well by matching use of the peppermint and the white alum. The peppermint and the white alum can be used in two ways, namely being edible and medicinal, can be used outside without direct contact with skin, and therefore toxic and side effects and bad stimulation on a human body can not happen.
CN103315972A Moxifloxacin hydrochloride tablets and preparation method thereof The invention discloses a preparation method of moxifloxacin hydrochloride tablets. The preparation method comprises the following steps of: (1) dissolving moxifloxacin hydrochloride in methanol, adding a disintegrating agent and evenly stirring; (2) crystallizing a mixed suspension in a particle-separation type cooling crystallizer and collecting particles; and (3) evenly mixing the particles with a filler and a lubricant which are pharmaceutically acceptable so as to obtain a mixture, and tabletting the mixture. The preparation method is simple in technology and the prepared tablet can be rapidly dissolved out and is invariable in color, good in stability and suitable for large-scale production.
US20080008764 Carbon-substituted diketopiperazine delivery systems Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and (b) a carrier of at least one mono-C-substituted or di-C-substituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.
CN1636570A Use of New Zealand vitexin-1 in preparing antiviral medicine The present invention discloses the use of New Zealand vitexin-1 in preparing medicine for resisting herpes simplex virus.
CN102204924A Application of compound 6-O-angeloylplenolin to pharmacy The invention discloses a natural compound 6-O-angeloylplenolin (6-OAP) and application of medicinal composition thereof to the preparation of medicaments for treating multiple myeloma (MM) and lung cancer. The 6-O-angeloylplenolin and the medicinal composition thereof can activate a check point of a cell spindle, induce retardation and apoptosis of a mitotic phase, have obvious cytotoxicity in multiple myeloma and lung cancer cells and have effective anti-tumor proliferation effect in a nude mouse myeloma transplantation model. As a natural compound, the 6-OAP has the advantage of promoting cytotoxicity in the multiple myeloma and lung cancer cells by cooperating with routine medicaments, such as adriamycin, dexamethasone, bortezomib and the like. The 6-OAP shows ideal pharmacokinetic characteristics in an SD mouse and reaches a new level in the aspect of tumor target of natural compounds. The 6-OAP can provide a new treatment medicament to patients with MM and medicament resistant tumors and has the advantages of moderate dose and cost, convenience in administration, obvious treatment effect, low toxic and side effects and the like.
CN101278944A Application of eggs rich in vanadium and chromium and method for producing the same The invention discloses an egg which is rich in vanadium and chromium and can treat diabetes mellitus and a manufacturing method thereof. The invention is characterized in that the vanadium comes from a vanadium compound which is added into basal diet for layer chickens and the chromium comes from a chromium compound which is added into the basal diet for the layer chickens. So the vanadium content of the basal diet is increased by 30ppm to 200ppm and the chromium content of the basal diet is increased by 1ppm to 80ppm. The layer chickens can eat the basal diet freely. After one week, eggs laid by the layer eggs are rich in the vanadium and the chromium. And the eggs have the advantages of good curative effect and little undesirable reaction.
US20050187275 Preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension; 3-(5-((3-chlorobenzyl)sulfanyl)-4-(3-methoxypropyl)-4H-1,2,4-triazol-3-yl)-N-(2-methoxybenzyl)propanamide The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.
CN102807620A Method for forming targeted chemotherapeutic agents for treating infectious and malignant diseases The invention provides a method for forming target chemotherapeutic agents for treating infectious and malignant diseases. A fusion protein is combined with a precursor drug for treating cancers. The fusion protein comprises (i) a ligand specifically bound to a growth factor receptor; (ii) a precursor drug enzyme by which a precursor drug can be transformed into an active pharmaceutical ingredient; and (iii) a linker positioned between the ligand and the precursor drug enzyme. The invention further provides a DNA construct which comprises (i) a nucleotide sequence coding the ligand specifically bound to the growth factor receptor, and (ii) a nucleotide sequence coding the precursor drug enzyme.
CN1970576A Extraction and preparation process of polysaccharide of Pteris semipinnata L. with anticancer activity The invention discloses an extracting making technique of phoenix-tail fern half-side flag polysaccharide with anti-tumour activity, which is characterized by the following: using hot water leaching method to obtain the product; possessing obvious anticancer action for SPCA-1, HL60 and CNE-2Z; inhibiting tumour for S180, liver cancer, lymphosarcoma and aldrine ascites carcinoma; improving tumour-inhibiting rate of animal transplanting tumour with 5-FU; lengthening lifetime; preparing random one agent of clinical acceptable pill, tablet, particle, capsule, injection and external skin agent.
EP0876387B1 Use of roxithromycin for the preparation of a medicament for improving the biological and antiviral activity of protease inhibitors Methods for improving the cellular uptake of protease inhibitors (e.g., HIV protease inhibitor), alone or in the presence of one or more additional therapeutic agents, in protease inhibitor-based therapies, involving administration of one or more AAG-binding compounds, such as macrolide or lincosamide antibiotics, which have sufficient binding affinity for AAG to competitively bind AAG in the presence of the protease inhibitor.
US20110236478 Co-crystals and pharmaceutical formulations comprising the same An immediate release formulation of an active ingredient.
CN101792474A Novel AzalomycinF microlide compounds and preparation method thereof and application thereof The invention discloses novel AzalomycinF microlide compounds and a preparation method thereof and application thereof. The invention aims to provide novel compounds having a unique structure and having broad-spectrum yeast fungus, banana vascular wilt and root-knot nematode resistant activities. The compounds provided by the invention are characterized by the compounds having a framework structure of a formula I or formula II, wherein R1 in the formula I is alkanoyl or alkoxylacylacetyl, R2 is hydrogen or methyl, R3 is hydrogen or methyl; and in the formula II, R1 is the alkanoyl or the alkoxylacylacetyl, R2 is the hydrogen or the methyl, R3 is the hydrogen or the methyl.
US20120129806 Arginase inhibitors as therapeutics Compounds according to Formula I are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, D, W, X, Y, and Z are defined in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use in treating or preventing a disease or a condition associated with arginase activity.
EP1652931A2 Recombinant adenoviruses, preparation and uses thereof for the treatment and/or prevention ofs cancers Defective recombinant adenovirus contains a heterologous DNA sequence (I), the expression of which in a target cell contributes to the inhibition of cell division.
CN101058823B Method of preparing cytidine disodium triphosphate and application The invention relates to a manufacturing method of disodium cytidine triphosphate, which comprises the following steps: proceeding enzymatic conversation with CMP material; proceeding ion exchange column chromatography; separating and purifying. The enzymatic conversation reaction principle is that: brewers' yeast gets the needed enzyme liquid of the enzymatic conversation reaction; brewers' yeast produces a plurality of biological enzyme as sugar glycolysis enzyme and phosphorylase with high sugar glycolysis ability; the biological energy produced by glycolysis glucose with sugar glycolysis enzyme is transferred to cytidine monophosphate by ATP; cytidine monophosphate and phosphate radical combines to form cytidine triphosphate with the effect of phosphorylase. The method shapes low cost, simple operation, high production, high product purity by optimization, which comprises the following steps: getting enzyme liquid; proceeding enzymatic conversation by adding the main material cytidine monophosphate, monobasic potassium phosphate of proper quantity and glucose; getting product by deposition, ion exchange column chromatography, segregation, purification, refining and vacuum drying.
WO2012122414A2 Linear dispensing system with universal escapement A linear dispensing system is provided that includes a plurality of channels, a pair of parallel rails, a plurality of carriers and a plurality of linear motor modules. The channels are configured to hold inventory products at an orientation. The pair of parallel rails is disposed at a bottom portion of the channels. The carriers are slidably disposed on the rails and have a conveyor unit configured to pick the inventory product from the channels while substantially maintaining the same geometric orientation as in the channel. The linear motor modules are disposed between the parallel rails and aligned end to end. The linear motor modules are coupled with the carriers and configured to pass the carriers to an adjacent linear motor module. Each carrier delivers a plurality of selected products of varying shapes to a universal escapement structure where the products are labeled, imaged, verified and dispensed.
WO2010012459A3 A process for the preparation of solifenacin salts and their inclusion into pharmaceutical dosage forms The invention relates to the synthesis of solifenacin, the preparation of its salts and their inclusion into pharmaceutically acceptable dosage forms.
WO2009007747A2 Hydantoin derivatives used as mmp12 inhibitors The invention provides novel hydantoin derivatives; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use as MMP12 inhibitors.
WO2010030781A2 Aromatic carboxylic acid derivatives for treatment and prophylaxis of gastrointestinal diseases including colon cancer Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.
US6911444 Non-steroidal IL-5 inhibitors, processes and intermediates for their preparation and pharmaceutical compositions comprising said inhibitors The present invention relates to IL-5 inhibiting 6-azauracil derivatives useful for treating eosinophil-dependent inflammatory diseases, to processes and intermediates for their preparation as well as to pharmaceutical compositions comprising the said derivatives. It further relates to the use of such derivatives as a medicine, and to processes for marking a receptor or imaging an organ using the said derivatives.
CN101297873B Chinese and western compound medicament composition for preventing and controlling aquatic livestock hepatobiliary syndrome The invention relates to the field of aquaculture industry, in particular to a compound Chinese-western pharmaceutical composition for prevention and treatment for liver and gall bladder syndrome of aquatic animals. The compound Chinese-western pharmaceutical composition is characterized in that: the composition according to parts by weight is as follows: 200 to 400 parts of Chinese thorowax root, 300 to 400 parts of indigowoad leaf, 100 to 200 parts of rhubarb, 20 to 70 parts of motherwort herb, 10 to 30 parts of glucurolactone and 100 to 200 parts of starch. The compound Chinese-western pharmaceutical composition has great effects on prevention and treatment for the liver and gall bladder syndrome of the aquatic animals and no medicine residue.
CN101092402A New compound in sulfonyl ureas, and medicine use This invention relates to a novel sulfonylurea compound or its pharmaceutical salt, their preparation method and pharmaceutical application. The novel sulfonylurea compound or its pharmaceutical salt can be used in drugs for preventing and treating diabetes or other diseases. The compound can be manufactured into oral liquids, injections and external use preparations.
US20130012579 Anti-obesity Potential of Calebin A The present invention discloses the potential of Calebin A in inhibiting adipogenesis and applications thereof in obesity management. The present invention elucidates the potential of Calebin A to favorably modulate biochemical markers associated with obesity. Notable biomodulatory properties of Calebin A include inhibiting leptin production, increasing adiponectin expression and inhibiting local (adipocyte) and systemic inflammation caused by pro-inflammatory cytokines Tumor Necrosis Factor (TNF-α), Interleukin-6 (IL-6) and Interleukin-1 (IL-1β).
CN1923173B Anti-cancer drugs slow release agent comprising anticancer antibiotics and synergist thereof Disclosed is an anticancer slow release agent which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow releaseauxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer antibiotics are selected from Idarubicin, Valtaxin, Pirarubicin and Mitoxantrone, The anti-metabolite drugs are selected from Pemetrexed, Carmustine, Tegafur, Zalcitabine, Emtritabine, Galocitabine, Ibacitabine, Ancitabine, Decitabine, Flurocitabine, Enocitabine, Imidazoletabine, Capecittabine, Gemcitabine, Fludrarbine, Raltitrexed, Dexrazoxane, Cladribine, Nolatrexed and folic acid, The slow release auxiliary materials are selected from EVAc, Polifeprosan, sebacylic acid copolymer, lactic acid, the viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose. The slow release microspheres can also be prepared into slow release implanting agent for injection or placement in or around tumor.
WO2014087818A1 Orally administered liquid formulation An orally administered liquid formulation, characterized by being obtained by blending a) vitamin B2 or an orally administrable sale thereof, b) an herbal-medicine-derived component, c) 1-10 parts by mass of polyvinyl pyrrolidone with respect to 1 part by mass (raw herbal medicine amount) of the herbal-medicine-derived component, and d) 0.02-1.6 parts by mass of at least one species selected from gallic acid and a derivative thereof with respect to 1 part by mass of vitamin B2. This orally administered liquid formulation has the excellent stability of a vitamin B2 species and does not precipitate in a liquid formulation, and can be applied in the fields of medicine and food products.
CN103550171A Cefminox sodium composition freeze-dried powder injection for injection The invention provides a cefminox sodium composition freeze-dried powder injection for injection and relates to the field of medicines and medicine manufacturing technique. The cefminox sodium composition freeze-dried powder injection contains the following raw materials: by weight, 7.26-9.17 parts of cefminox sodium, 7.02-8.97 parts of chitosan nanoparticles and 81.38-87.10 parts of water for injection. The invention has advantages as follows: 1) the composition has a good antibacterial effect on klebsiella pneumonia, has sensitivity rate of 91.9%, and has obvious advantages in resisting ESBLs-producing klebsiella pneumonia; 2) the concentration of active ingredients of the composition is increased in a central compartment and cycling time is prolonged such that the medicine can play a better role in systemic treatment and curative effect of the medicine in a focus target site can be enhanced; 3) stability of the freeze-dried powder injection against beta-lactamase generated by gram-negative bacteria is enhanced, and distribution in vivo is good; 4) activity is enhanced such that medicine treatment cycle is shortened and possibility of adverse reaction caused by accumulation of cefminox sodium is reduced; and 5) the chitosan nanoparticles can replace mannitol to be used as a freeze-drying skeleton agent of the freeze-dried powder injection so as to eliminate the active effect of mannitol on human body.
US8378118 Pyrazole-based thyroid receptor compounds The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.
US20050234090 Modulators of chemokine receptor activity Chemokine receptor antagonists, in particular, bicyclic diamine compounds of Formula (I) that act as antagonists of chemokine CCR2 and CCR3 receptors including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leucocyte accumulation are described herein.
EP2536413A1 Use of synthetic polysulphated oligosaccharides as cleaning agents for a wound The present invention relates to the use of at least one compound selected among the synthetic polysulphated oligosaccharides having 1 to 4 ose units and to the salts and complexes thereof as cleaning agents for a wound. The invention can be used in particular for preparing bandages intended for cleaning wounds.
EP2548874A2 Substituted piperazines as CB1 antagonists Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB, receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
US20110081413 Pharmaceutical Compositions Comprising Phosphate-Binding Polymer The present invention discloses pharmaceutical composition comprising phosphate binding polymers such as Sevelamer carbonate substantially free of monovalent anion other than bicarbonate anion. Particularly, monovalent anion content is less than about 0.05% (w/w). Disclosed are compositions comprising wet granulated Sevelamer carbonate free of added metal ions and/or added monovalent anion source.
US7026289 Method and compositions for treating hyperlipidemia and other conditions The present invention relates to a method of treating hyperlipidemia and to reducing triacylglycerols, glycerol and cholesterol in a patient. The method includes the step of administering a therapeutically effective amount of a type-5 selective somatostatin agonist to said patient. A pharmaceutical composition comprises said agonist and such product is used in the preparation of the composition for use in treating hyperlipidemia or reducing triacylglycerols, glycerol and cholesterol in a patient's body.
WO2010055164A2 Novel inhibitors of flavivirus replication The present invention relates to a series of Isoquinolone derivatives which are suitable to treat infections with viruses belonging to the family of the Flaviviridae and more preferably infections with Hepatitis C virus (HCV). The present invention also relates to Isoquinolone compounds for use as a medicine for the prevention or treatment of viral infections, preferably infections with viruses belonging to the family of the Flaviviridae.
EP1083887B1 Pharmaceutical compositions for the treatment of ulcers Pharmaceutical compositions for the therapy and the prevention of ulcer and dyspepsia relapses comprising as essential components the following components a) and b): component a): one or more components selected from the conventional anti-ulcer products; component b): organic compounds containing the -ONO2 function, or inorganic compounds containing the -NO group, characterized in that they are NO nitric oxide donors.
CN1562047A Glycerin invert sugar injection A high-safety glycerine invertose injection is prepared from glycerine, glucose, pectose and water.
WO2011075462A1 Agent that interacts with serum amyloid a gene for the treatment of glaucoma The present invention provides compositions and methods for treating glaucoma, methods for diagnosing glaucoma, and methods for identifying agents which may be useful in the treatment of glaucoma. More specifically, the present invention describes the use of agents that modulate the expression of serum amyloid A, wherein such agents are inhibitors of p38 MAPkinase.
EP2222631A2 Substituted phenylmethyl bicyclocarboxyamide compounds This invention provides a compound of the formula (I). These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.
CA2294274C Compositions and methods for reversibly increasing permeability of biomembranes A pharmaceutical composition for the permeabilization of biological membranes comprising a pharmaceutically effective amount of a compound of the general formula: (see formula I) wherein R denotes a saturated or unsaturated chain of between 4 to 10 carbon atoms and R' denotes a saturated or unsaturated chain of between 5 and 30 carbon atoms, their salts, esters or amides in a pharmaceutically acceptable carrier. A method of enhancing permeabilization of a biological membrane comprising exposing the membrane to a compound of the general formula II: (see formula II) wherein R denotes a saturated or unsaturated chain of between 1 to 10 carbon atoms and R' denotes a saturated or unsaturated chain of between 5 and 30 carbon atoms, their salts, esters or amides.
EP2650021A1 Medical device for controlled release of drug The purpose of the present invention is to provide a medical device for the controlled release of a drug suitable for an ophthalmic lens that, compared to a conventional contact lens for controlled release of a drug, releases a reduced initial controlled longer-release amount of the drug retained in the device and as a result, thus enabling longer-term controlled release of the drug in a therapeutically effective dose, such device having the same oxygen permeability as that a conventional SHGCL. The foregoing is accomplished by a medical device for the controlled release of a drug comprising an amphiphilic hydrogel that retains a drug, where the rate of controlled release of the drug is 50 wt% or less 24 hours after drug release is initiated.
CN101961328A Application of sodium houttuyfonate as synergist of antifungal medicament The invention relates to the technical field of medicaments, in particular to novel application of sodium houttuyfonate as a synergist of an antifungal medicament. The antifungal medicament is an azole or polyene antifungal medicament; and 1 to 16mu g of sodium houttuyfonate is added into each 1ml of antifungal medicament. Experiments prove that: when the sodium houttuyfonate is combined with the antifungal medicament such as fluconazole, ketoconazole, miconazole or amphotercin B, and the like, the treatment effect of the sodium houttuyfonate on superficial or deep fungal infection can be ensured under the condition of reducing the dosage and the sodium houttuyfonate can make the antifungal medicament recover the effect on medicament-resistant fungi, so the sodium houttuyfonate can be used as the synergist of the antifungal medicament. The sodium houttuyfonate serving as the synergist of the antifungal medicament can reduce the dosage of the azole or polyene antifungal medicament so as to reduce the toxic and side effects of the medicament; and particularly, the sodium houttuyfonate makes the antifungal medicament recover the effect on the medicament-resistant fungi, effectively treats fungal infection, particularly medicament-resistant fungal infection, and has important clinical application value.
WO2014090583A1 Delphinidin for combating melanoma cells The invention relates to a composition comprising a complex of delphinidin and a sulfoalkyl ether-β-cyclodextrin for use in the treatment of malignant melanoma.
US20080269487 6-{[1-(carbamoylmethyl)piperidin-4-yl]oxy}-4-(3-chloro-2-fluoroanilino)-7-methoxyquinazoline; prevent, treat tumours which are sensitive to inhibition of erbB receptor tyrosine kinases The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, R1 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.
CN101045040A Wrapped tablets dichlororeytadin and its preparing method A coated Desloratadine tablet features that it contains beta-cyclodextrin and leucine for preventing its degradation in oxygen and moisture, resulting in high stability. Its preparing process is also disclosed.
CN102579371A Gemcitabine hydrochloride freeze-dried powder injection The invention relates to a gemcitabine hydrochloride freeze-dried powder injection, and further relates to a preparation method of the gemcitabine hydrochloride freeze-dried powder injection, as well as application of the gemcitabine hydrochloride lyophilized powder injection in preparing medicines for treating non-small-cell carcinoma, pancreatic cancer and the like in middle and late stages.
CN1923286A Anticancer slow release agent of anticancer antibiotics and its progression agent Disclosed is a compound anticancer slow release agent which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant, The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the anticancer active constituents include anticancer antibiotics and/or anticancer antibiotic synergistic agent, the slow release auxiliary material is selected from ethylene-vinylacetate copolymer, polifeprosan, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid) copolymer, poly(fumaric acid-sebacylic acid) copolymer, the slow release microspheres can also be prepared into slow release implanting agent for lowering down the whole body toxicity reaction of the anti-cancer medicament, selectively increasing the tumor local medicinal concentration, and improving the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation.
DE102006030073A1 Lipstick, useful for the treatment of herpes, protection of lip from sunburn and for lip care Lipstick (I) for the treatment of herpes, protection of lip from sunburn and for lip care.
CN101955477A 2-cyclopropyl-4-substituted thiophenyl quinoline compounds as well as intermediate, preparation method and application thereof The invention discloses 2-cyclopropyl-4-substituted thiophenyl quinoline compounds represented by the formula A as well as a pharmaceutically accepted solvate, an optical isomer or polymorph and a reaction intermediate compound thereof represented by the formula D, wherein R1 is H, halogen or C1-C4 alkoxy; R2 is H, halogen or group represented by the formula Q; and R is H, halogen, C1-C4 alkyl or C1-C4 alkoxy. The invention also discloses a preparation method and application of the compounds in the preparation of medicines for inhibiting HMG-CoA reductase and treating hyperlipidaemia related diseases. Compared with the existing pitavastatin, rosuvastatin and atorvastatin in the prior art, most of the 2-cyclopropyl-4-substituted thiophenyl quinoline compounds can better or at least equivalently inhibit the activity of HMG-CoA reductase and can be used for treating hyperlipidaemia related diseases.
US20080287457 Inhibitors of Akt Activity The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.
CN103099811A Chicken coccocidiosis preventing and treating composition The invention belongs to a chicken coccocidiosis preventing and treating composition in veterinary drugs. The chicken coccocidiosis preventing and treating composition is composed of the effective component by weight: 80% of xytetracycline hydrochloride and 20% of trimethoprem. The veterinary drug composition is used for treating the coccocidiosis and the bacterial diseases of chicken, and the cure rate is above 96%. The process for processing the composition comprises accurately weighing all of the effective components dried previously, mixing, weighing and packaging, testing quality and warehousing. The method of using the composition comprises mixing the composition with other materials by the proportion of 0.05-0.1%. The composition is applied continuously for 3-5 days as a course of treatment.
CN101327185A Anticancer sustained-release implantation agent An anticancer sustained-release implant is characterized in that active anticancer ingredient is wrapped into pharmaceutical excipient to be made into the sustained-released implant or sustained injection. The active anticancer ingredient is the combination of anti-metabolism anticancer medicine and synergistic agent thereof. The synergistic agent is made from mustine drug and/or antimitotic drug and/or plant alkaloids. The pharmaceutical excipient is made from polylactic acid, copolymer of polyglycolic acid and glycolic acid, ethylene-vinyl acetate copolymer, FAD: sebacic acid (SA) copolymer and/or polifeprosan, etc. The sustained-release injection is composed of sustained release microspheres and menstruum, and the menstruum is classified into common menstruum and special menstruum with suspending agent. The suspending agent is made from sodium carboxymethyl cellulose, mannite, etc. and is used for suspending active anticancer ingredients or sustained-release gains or microspheres containing active anticancer ingredients so as to facilitate injection. Partial tumor placement or sustained-release agent injection can reduce medicine systemic toxicity effect as well as can selectively increase medicine concentration at partial tumor to enhance the curative effect of non-operative treatments such as chemotherapeutic drug, radiation therapy, etc.
WO2013062071A1 Piperazine derivative and salt thereof Provided are: a novel compound represented by formula (I) and having an Akt inhibitory activity and a cell proliferation inhibitory activity or a salt thereof; and a medicinal agent useful for the prevention and/or treatment of cancer, which relies on the above-mentioned activities. [In the formula, R1 and R2 independently represent a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, an alkyl group or the like; R3 represents an aromatic hydrocarbon group, a saturated or unsaturated heterocyclic group; R4 and R5 independently represent a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, an alkyl group, an alkynyl group, a cycloalkyl group, an aromatic hydrocarbon group, a saturated or unsaturated heterocyclic group or the like; and R6 represents a hydrogen atom, a halogen atom, an amino group, an alkyl group or the like, wherein each of the combination of R1 and R2, the combination of R4 and R5 and the combination of R5 and R6 may, in conjunction with an atom to which both of the variables bind, together form a ring, and wherein a case in which each of R4 and R5 represents a hydrogen atom is excluded.]
CA2858192A1 Medical food for the dietary management of depression and anxiety and methods thereof ?The present invention relates to medical food for the dietary management of depression and/or anxiety comprising a water containing from 0.0002 to 0.0278 mol.% of isotopologue HOD, preferably, from 0.0178 to 0.0278 mol.% of isotopologue HOD. Further, the present invention relates to method of the dietary management of depression and/or anxiety comprising a step of administering to a subject in need thereof the medical food of the invention. Further, the present invention relates to method of the treatment of depression comprising steps of administering to a subject an antidepressant drug and administering to the subject the medical food of the invention. Further, the present invention relates to method of the treatment of anxiety comprising steps of administering to a subject an antidepressant drug and administering to the subject the medical food of the invention.
US20110071102 Compositions and Methods to Treat Recurrent Medical Conditions The invention describes methods and compositions for alleviating recurrent medical afflictions for which anxiety may cause or exacerbate the affliction. A subject suffering from the affliction is treated with a combination of a pharmaceutical that enhances learning, and a second pharmaceutical recognized to be useful for treatment of the affliction. Representative afflictions include insomnia, erectile dysfunction, female sexual dysfunction, neuropathic pain, attention deficit disorder, and depression.
CA2168937C Anti-neurodegeneratively active 10-aminoaliphatyl-dibenz[b,f]oxepines Base-substituted dibenz[b,f]oxepines of formula I (see formula I) wherein alk is a divalent aliphatic radical, R is an amino group that is unsubstituted or mono- or di-substituted by monovalent aliphatic and/or araliphatic radicals or disubstituted by divalent aliphatic radicals, and R1, R2, R3 and R4 are each, independently of the others, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and pharmaceutically acceptable salts thereof, may be used as anti-neurodegenerative active ingredients of medicaments. The invention relates also to novel compounds of formula I.
US20100190684 Inhibition of palmitoyl acyl transferase expression and/or activity for the regulation of antiproliferative factor activity The invention generally concerns inhibition of a molecule that has a role in post-translational modification of a receptor for antiproliferative factor (APF) of bladder epithelial cells, thereby modulating the APF. In particular, inhibition of DHHC2 activity and/or ZDHHC2 expression results in modulation of APF receptor activity, and in specific aspects such modulation is therapeutic and/or preventative for a bladder condition, such as interstitial cystitis. In addition, inhibition of CKAP4 palmitoylation in certain cases also decreases its activity as a tPA receptor on smooth muscle cells or surfactant A on type II pneumocytes, and/or generally inhibits its function as a cell membrane receptor, cell chaperone molecule, and/or membrane trafficking agent.
US7262221 Hydrophobic core coupled to plurality of hydrophilic moieties that form micelles in solution; encapsulate lipoproteins; atherosclerosis; cardiovascular disorders The present invention provides polymeric compounds that can form micelles in solutions. These compounds have a hydrophobic, core that is coupled to a plurality of hydrophilic moieties.
WO2011018506A1 miRNA COMPOUNDS FOR TREATMENT OF PROSTATE CARCINOMA The invention inter alia relates to new pharmaceutical compositions comprising miRNAs mi R-130a, mi R-203 and miR-205,and their use for the treatment of cancer, in particular prostate cancer. F 8812 / DB
US20120283284 Melonine bisindole compounds, pharmaceutical compositions, preparation method and use thereof The present invention relates to pharmaceutical technical field, to melonine bisindole compounds, pharmaceutical compositions thereof, and preparation methods thereof. Specifically, the present invention relates to melonine bisindole compounds of Formula I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts thereof. The present invention further relates to method for preparing the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof, and the use of the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of cancers.
US20100152146 Topical Administration of Danazol Pharmaceutical preparations for topical or local administration of drugs directly to the skin for treatment of disorders of the subcutaneous fatty tissue, in particular in cases of cellulite, are disclosed herein. In a preferred embodiment, the drug is danazol or gastrinone. In another embodiment, the drug is danazol in combination with an aromatase inhibitor or an estrogen compound. The preferred formulations contain drugs in the form of micro or nanoparticles, which may be formed of drug alone or in combination with an excipient or carrier. The excipient or carrier may modify the release rates or enhance absorption into the affected area. The drug formulation may be in the form of a cream, lotion, ointment, gel or emulsion, solution or foam.
US20090221684 Molecules for Gene Delivery and Gene Therapy, and Methods of Use Thereof One aspect of the present invention relates to a synthetic non-viral vector composition for gene therapy. Another aspect of the invention relates to the use of the composition for in vitro, ex vivo and/or in vivo transfer of genetic material. The invention also encompasses a pharmaceutical composition (useful for delivery of nucleic acids to a cell), containing a non-cationic amphiphilic molecule or macro-molecule; or a cationic amphiphilic molecule or macromolecule that transforms from a cationic entity to an anionic, neutral, or zwitterionic entity upon a chemical, photochemical, or biological reaction. Another aspect of the invention relates to multicationic compounds that are composed of three or more amino acids. The present invention also relates to the use of the pharmaceutical composition for delivery of nucleic acids to a cell. Moreover, the invention encompasses the non-viral vector compositions tethered to a surface. The surface-tethered compositions are useful for the delivery of nucleic acids to cells in contact with the surface. An additional embodiment of the invention relates to a hydrogel comprising a composition of the invention, and methods of using same for the delivery of genetic material to a cell.
WO2014028829A1 Novel kappa opioid ligands The invention provides novel ligands of Kappa (κ) opioid receptors, such as can be used to modulate a Kappa opioid receptor. Methods of synthesis and methods of use are also provided. Compounds of the invention can be used therapeutically in the treatment of dissociative disorders or pain, or to provide neuroprotection, or to induce diuresis, or to modulate the immune system, or for treatment of one or more of an affective disorders comprising depression or stress/anxiety; an addictive disorder; alcoholism, epilepsy; a cognition deficiency; schizophrenia; Alzheimer's disease; or pain.
US20080248139 adding an effective amount of p-pivaloyloxyferutinine to an acceptable excipient for a cosmetic or dermatological composition The invention relates to a process for the preparation of ferutinine (Ia) from Ferula spp extracts comprising basic hydrolysis of the extracts and treatment with p-pivaloyloxybenzoic acid. The invention relates also to the use of the extracts and ferutinine in the cosmetic and dermatological field.
CN103505465A Anti-thrombus medicinal composition containing dabigatran etexilate The invention relates to an anti-thrombus medicinal composition containing dabigatran etexilate, which is characterized by consisting of an active component dabigatran etexilate and an anti-thrombus medicine and being configured to contain 0.1-500mg of active ingredient in each unit dosage, wherein dabigatran etexilate and aspirin exist at a molar ratio (aspirin to dabigatran etexilate) of 2.5-11.5, and the anti-thrombus medicine is aspirin. The two components exist in a free state or in a pharmaceutically acceptable salt form. Astonishingly and unexpectedly, the combination of dabigatran etexilate and aspirin is proved to generate the synergistic effect of the two active components. The medicinal composition is used for treating embolism-related thromboembolism diseases after embolism, thromboembolism diseases related to atrial fibrillation or thromboembolism diseases related to the application of vascular repair.
US20060034957 Vitamin-containing system for stabilising the immune response of animals A vitamin-containing system for stabilising the external and the internal immune response of animals consists of two parts or “kits” to be used successively or separately, one mainly including biotin and the other mainly including vitamins E and C. Both kits include allicin and crushed radishes and are mixed in a carrier. The system is used for prophylactic or curing treatment of a number of diseases in animals, especially in farming stocks.
CN101518325A Edible health-care salt and method for preparing same The invention relates to an edible health-care salt and a method for preparing same. The salt is prepared by the following methods: firstly, mixing the salt with ferrous sulfate by the weight ratio of (500-600): (1-20) and heating the mixture to the temperature of 810-870 DEG C; secondly, stirring the mixture for 20-30 minutes at the constant temperature; subsequently, stopping the heating and naturally cooling the salt, thus obtaining mixed solid matter; finally, grinding and filtrating the mixed solid matter by a screen of 120-160 meshes, thus preparing the edible health-care salt. The edible health-care salt has lower price, greatly reduces the cost, is innocuous and harmless, has no stimulation effect to the human body, complies with the quality and safety authorization requirement in the health-care product field, is immensely popular with vast consumers and patients, is convenient for popularization, has safe and relatively comprehensive health-care function and is suitable for normal groups.
CN101036719B Sirup agent for curing cough for children and the preparing method The invention discloses a syrup for treating cough in children which is formed by materials of 50-400 ml licorice fluidextract, 10-60 ml balloonflower root fluidextract, 2-20 g ammonium chloride, 10-40 ml orange tincture, 200-500 g saccharose and 3-7 g sodium benzoate, and a method for preparing the same. Compared with the existing technology, the syrup of the invention can not only eliminate phlegm and relieve cough with exact curative effect for cough caused by cold of children, but also can reduce content of saccharose in the preparation to solve problem that it is too sweet of the syrup for treating cough in children to be taken for part patients, thus the syrup is more convenient for being taken for children, as well as can avoid anxiety, lack of concentration, hyper-sensitive in children which may be caused by increasing of children epinephrine level due to too much saccharose content.
WO2009018169A1 Substituted cyclohexanols Disclosed herein are substituted cyclohexanol opioid receptor modulators and/or neurotransmitter reuptake modulators of Formula I or Formula II, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
WO2006055964A3 Zolmitriptan crystal forms The invention encompasses novel crystalline forms of zolmitriptan herein defined as Form B, D, C, E, F, G, H, I, J, K, M, N, O, P, Q, R, S, or Amorphous and to methods of making thereof. The invention also encompasses methods of making zolmitriptan crystalline Form A.
EP1243583B1 Heterocyclic compounds having sulfonamide groups Heterocyclic compounds having sulfonamide or sulfonylurea groups, specifically heterocyclic compounds of general formula, pharmacologically acceptable salts of the same, or hydrates of both: (|) wherein A is hydrogen, halogeno, optionally halogenated C1-4 alkyl, or the like; B is optionally substituted aryl, monocyclic heteroaryl, or the like; K is a single bond or the like; T, W, X and Y are each independently =C(D) - (wherein D is hydrogen, halogeno, or the like) or nitrogen; U and V are each independently =C(D) -, nitrogen, oxygen, or the like; Z is a single bond or -CO-NH-; and R1 is hydrogen or the like.
EP2406227A1 Process for manufacturing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1- hydroxyethyl)-8-hydroxyquinolin-2(1h)-one. A process for preparing the compound of formula (I), or a Pharmaceutically acceptable salt thereof, (I) which process comprises: reacting, in a xylene solvent, a compound of formula (V) with the compound of formula (IV) to give a compound of formula (III) followed by a P1 deprotection step and a P2 deprotection step.
US20070293563 Novel Agents for Preventing and Treating Disorders Connected to Impaired Neurotransmission The present invention refers to coumarin ethers of the formula (I), wherein R1 is H, OH or (E)-3-methyl-but-2-enyl, R2 is selected from the group consisting of methyl, 3-(4,5-dihydro-5,5-dimethyl-4-furanon-2-yl)-2-(E/Z)-butenyl, (E/Z)-3,7-dimethylocta-2,6-dienyl, 7-hydroxy-3,7-dimethyl-2-octen-6-on-yl and (E/Z, E/Z)-1-acetyl-oxy-3,7,11,11-tetramethyl-undeca-2,7-dien-10-on-yl, R3 is H, R1 and R2O together for the group —O—C(C(═CH2)CH3)H—CH2—O— or the group —C(H)═C(H)—C(CH3)2—O— or R2O and R3 together form the group —O—C(H)(C(CH3)2(H)—O—C(O)CH3)—CH2—, preferably to obliquin, for use as medicaments, especially for the treatment and/or prevention of disorders connected to impaired neurotransmission, as well as to dietary and pharmaceutical compositions and plant extracts containing such coumarin ethers and their uses.
CN101204391A Isoflavone compound curing atherosclerosis through strengthening reverse cholesterol transport mechanism and composite thereof The invention relates to the application of isoflavones red clover (form 1) and genistein (form 2). The invention is utilized for the preparation of medicine through strengthening the reverse cholesterol transport processed treatment and/or preventing the atherosclerosis. The medicine of strengthing the reverse cholesterol transport processed treatment and/or preventing the atherosclerosis comprises the medicine presented the liveness through the up-regulation of the high density lipoprotein receptor CLA-1/SR-BI and the ATP cassette antigen ABCA1. The invention also relates to the drug composition of strengthening the reverse cholesterol transport processed treatment and/or preventing the atherosclerosis, the active constituents efficient chosen from the isoflavones red clover (form 1) and genistein (form 2) provided on the drug composition and optional carrier which is able to be adopted by the pharmacy.
US20080138398 Dual release nicotine formulations, and systems and methods for their use This invention relates generally to a method to provide habitual tobacco users with products, methods and apparatus to reduce and eventually terminate their dependence on nicotine containing products. More specifically, the invention relates to a nicotine-based medicament that is formulated in such a way as to effectively reduce or eliminate the sensations of craving associated with addictive nicotine use.
WO2003006628A3 Nad synthetase inhibitors and uses thereof Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1-X-Ar2-Y-L-Z-Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof. Also disclosed are methods which involve the use of the compounds of the present invention, for example, in treating or preventing a microbial infection in a mammal or plant, killing a prokaryote or decreasing prokaryotic growth, disinfecting a material or environment contaminated by a microbe, increasing food animal production, controlling harm to plants by a pest or insect and combating agroterrorism. Examples of microbes affected by the compounds of the present invention are bacteria and fungi.
CN1748694A Albendazole nasal jelly for treating allergic rhinitis The present invention relates to the preparation process of nasal albendazole jelly and the application of the nasal albendazole jelly in treating allergic rhinitis.
CN103319367A Caproamide derivative, and preparation method, intermediate and application thereof The invention discloses a caproamide derivative represented by formula A or a pharmaceutically acceptable salt thereof, wherein R1 is H or halogen; R2 is halogen, or C1-C4 alkyl, C1-C4 alkoxy, or a C3-C7 heterocyclic ring, the number of heteroatom in the heterocyclic ring is 1-3, and the heteroatom is nitrogen and/or oxygen; R0 is benzyl, substituted benzyl or C4 alkyl, and a substituent of substituted benzyl is C1-C3 alkyl. The invention also discloses a preparation method, an intermediate and an application of the caproamide derivative. The caproamide derivative provided by the invention has effective and better antibacterial function, and has higher application value in the medical field.
US7375222 anti-dementia agent which uses a BEC 1 potassium channel inhibitor as the active ingredient; to improve learning disorder This invention relates to an anti-dementia agent which uses a BEC 1 potassium channel inhibitor as the active ingredient. It was proved that the BEC 1 potassium channel inhibitor has an action to improve learning disorder and is useful as a preventive or therapeutic agent for diseases, preferably dementia, in which the BEC 1 potassium channel is considered to be concerned. Illustratively, it was confirmed by an in vivo test that the BEC 1 potassium channel inhibitor has an action to improve learning disorder. Also, it was found that a compound having 2,4,6-triamino-1,3,5-triazine has a BEC 1 potassium channel inhibitory action.
CN103130865A Sophocarpidine, oxymatrine glycyrrhetinic acid double salt, and preparation method and use thereof The invention relates to a compound of sophocarpidine and glycyrrhetinic acid double salt, a compound of oxymatrine glycyrrhetinic acid double salt, and a composition, a preparation method and use thereof, and particularly relates to the use of two double salts in the treatment of inflammation, bacterial infected skin diseases and allergic dermatitis. The polarity of the glycyrrhetinic acid, easy oxidation of sophocarpidine, and strong moisture adsorption of oxymatrine are well improved by the sophocarpidine glycyrrhetinic acid double salt; the preparation method is simple and easy to operate, and is high in yield; meanwhile, a good synergistic effect is displayed in anti-inflammation and antibiosis; and the dosage is obviously reduced.
WO2013146435A1 Agent for preventing or treating giant cell tumor or chondrosarcoma arising in bone/soft tissue The present invention provides, inter alia, an agent for preventing or treating a giant cell tumor or chondrosarcoma arising in bone/soft tissue, the agent containing a non-steroidal anti-inflammatory drug or thiazolidine derivative as an active ingredient.
US7029663 substantially anhydrous, using hydrocarbon gel and/or petrolatum as a base; increased storage stability A substantially anhydrous stable ointment containing Aspirin which is characterized in using gelation hydrocarbon and/or vaseline as a base. The ointment is superior in stability and can be stored for a long term.
WO2008128982A1 Thioxoquinazolinone derivatives as glutaminyl cyclase inhibitors The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: R1 represents (A) or (B) and R2, R3, R4, R5, R6, X1, X2, X3, X4, Y and Z are as defined throughout the description and the claims.
US20110123574 Inhalable sustained therapeutic formulations The present invention is based, in part, on the unexpected discovery that particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that comprise a phospholipid and a sufficient amount of leucine can produce sustained effect of the agent. Specifically, particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that contain a phospholipid or combination of phospholipids, wherein the phospholipid or combination of phospholipids is present in the particles in an amount of about 1 to 46 weight percent; and leucine, wherein leucine is present in the particles in an amount of at least 46 weight percent, can contribute to sustained effect of the agent. Particles that comprise at least 46 weight percent leucine but that do not contain phospholipids do not exhibit these same sustained effect properties.
US7465722 Biphenyl vasopressin agonists A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.
EP2130824A1 Composition for treating infectious diseases caused by helicobacter The invention relates to a compound of general formula (I) for use in a pharmaceutical composition for treating infectious diseases caused by Helicobacter pylori. R1 and R2 are O, S or N, and can be identical or different; R3 is O or S; R4 is H or a (C1-C6) alkyl group; n represents a value between 0 and 3; and R5 is an NO2, COOR' or So3R' radical wherein R' is a hydrogen (H) atom or a (C1-C6) alkyl group.
US20100272655 Menthylcarboxamides and Their Use as Cooling Agents Described is a new cooling agent represented by Structure I and compositions with known coolers having cooling properties and the application of Structure I in foodstuffs and chewing gum:
CN103751162A Application of benzyl-4-hydroxy-3,5-dimethoxy benzoate in preparation of drugs for treating acute inflammation The invention relates to the field of drugs, and particularly relates to a compound capable of inhibiting proteasomes and relieving damage of an acute inflammatory reaction to bodies. The compound has the molecular structure of benzyl-4-hydroxy-3,5-dimethoxy benzoate, can increase the survival rate of endotoxic shock mice in in-vivo tests, and has potential new drug development value.
CN101401845A Liniment for treating toothache The invention relates to a medicament for treating toothache, and in particular to a liniment for treating the toothache. The liniment adopts the technical proposal that the liniment comprises the following raw materials in weight portion: 50 to 60 milligrams of cassia powder, 250 to 300 milligrams of honey and 5 to 10 milligrams of metronidazole. The raw materials are mixed evenly and then smeared on the toothache part. The medicament has the advantages of anti-inflammatory analgesic, efficacy of nourishing gum, simple preparation, and low cost.
US7067516 Compounds used as antiinflammatory agents and enzyme inhibitors Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
WO2013075176A1 Compositions and methods for modulating uterine contractions Provided herein are methods for stimulating or inducing contractility of myometrial tissue, methods for inducing or stimulating uterine contractions, and methods for inducing or assisting labour in pregnant subjects, comprising exposing myometrial tissue to an effective amount of an agent capable of inhibiting the expression or activity of an ERG potassium channel, or a homologue thereof.
CN101559076B Anti-tumor-stroma metalloprotease inhibitor The invention discloses a use of third-valence metal salt as MMPs inhibitor, the third-valence metal salt is free third-valence metal salt or third-valence metal composition. The third-valence metal salt is third-valence rare earth salt or third-valence transition metal salt or third-valence major-group metal salt. Compared with prior MMPs inhibitor, the third-valence metal salt of the invention has relatively strong MMPs inhibiting activity; furthermore, the third-valence metal salt of the invention has simple structure, low cost and convenient availability.
WO2007073646A1 The application of 2-bromide-isovanillin for the manufacture of a medicament for anti-cancer or/and radiation, chemotherapy sensitization The application of 2-bromide-isovanillin for the manufacture of a medicament for anti-cancer or/and radiation, chemotherapy sensitization is provided. The medicine comprising 2-bromide-isovanillin used as the active component for anti-cancer or/and radiation, chemotherapy sensitization has the following features: 1) low toxicity ,and no obviously adverse reaction; 2) significant curative effect, and having conspicuous inhibiting and promoting apoptosis effect on tumor cell proliferation; 3)having broad spectrum anticancer activity; 4)combination administration with anti-metabolism chemotherapeutic medicine for synergy and attenuation, and lowing the multidrug resistance of chemotherapeutic medicine; 5) oral administration as the main route of administration, convenience and safety.
WO2013090833A8 Angiotensins for treatment of fibrosis The present invention provides, among other things, methods and compositions for treating or preventing fibrotic diseases, disorders or conditions based on Angiotensin (1-7) polypeptides, and analogs or derivatives thereof. In some embodiments, compositions and methods for treating or preventing pulmonary fibrosis, pulmonary hypertension, chronic obstructive pulmonary disease (COPD), asthma, cystic fibrosis, kidney fibrosis, liver fibrosis, systemic sclerosis, post-surgical adhesions, accelerating wound healing, and reducing or preventing scar formation are provided.
US7037928 Compositions of N-(methylethylaminocarbonyl)-4-(-3-methylphenylamino)-3-pyridylsulfonamide and cyclic oligosaccharides The invention relates to compositions of N-(1-methylethylaminocarbonyl)-4-(3-methylphenylamino)-3-pyridylsul fonamide and cyclic oligosaccharides with increased release, to methods for their preparation, to pharmaceutical froms containing them as well as to their use.
CN1785183A Injection used for improving immunity of human An injection for improving human immunity features that it contains levamisole (0.05-5 wt%). It can improve the immune function of cells and body fluid, so it can be used as the immune synergist.
US20070248659 Individualized cancer therapy In certain preferred embodiments, the invention provides methods for treating cancer, which comprise (a) obtaining a specimen of cancer tissue from a patient; (b) obtaining a specimen of normal tissue in the proximity of the cancer tissue from such patient; (c) extracting total protein and RNA from the cancer tissue and normal tissue; (d) obtaining a protein expression profile of the cancer tissue and normal tissue using 2D DIGE and mass spectrometry; (e) identifying proteins that are expressed in such cancer tissue at significantly different levels than in the normal tissue; (f) obtaining a gene expression profile of the cancer tissue and normal tissue using microarray technology and comparing the results thereof to the protein expression profile; (g) prioritizing over-expressed proteins by assessing the connectivity thereof to other cancer-related or stimulatory proteins; (h) designing an appropriate RNA interference expression cassette to, directly or indirectly, modulate the expression of genes encoding such prioritized proteins; (i) incorporating said cassette into an appropriate delivery vehicle; and (j) providing the patient with an effective amount of the delivery vehicle to, directly or indirectly, modify the expression (i.e., production) of such proteins.
CN101543498B Application of bitter theophylline in preparing anti-inflammation and analgesic drugs The invention discloses an application of bitter theophylline in preparing anti-inflammation and analgesic drugs. The bitter theophylline is extracted from the C. Kucha (Chang et Wang) Chang. The C. Kucha (Chang et Wang) Chang is extracted by water after being dried by the fixation pan. The lead subacetate makes the tea polyphenol precipitate. The chloroform extract is chromatographied by silica gel column and recrystallized, then the bitter theophylline with the purity of over 95 percent can be got. The experiment that the formaldehyde makes the foot of the mouse swell and the experiment that the xylene makes the ear of the mouse swell show that the swelling foot and ear of the mouse can be obviously controlled by giving bitter theophylline of 32 mg per kilogram and 64 mg per kilogram. The experiment that acetic acid causes the body twist of the mice shows that 8 mg per kilogram to 64 mg per kilogram of bitter theophylline have obvious analgesic effect. The experiment that the hot plate makes the mice feel painful shows that 64 mg per kilogram of bitter theophylline have the obvious analgesic effect after 30 minutes. The above experiments show that bitter theophylline can be usedto prepare anti-inflammation and analgesic drugs.
CN1876658A Gambogicacid derivative and its preparation method and uses in pharmacy The invention discloses the preparing method and application of cambogic acid derivation. The cambogic acid derivation is made by nitric oxide donator and cambogic acid. The cambogic acid derivation has the antineoplastic action.
CN1679912B Extraction of liuwei Dihuang polysaccharide, products and use thereof A process for preparing the polyose from 6 Chinese-medicinal materials: prepared rehmannia root, dogwood fruit, yam, alismatis rhizome, tuckahoe and tree peony bark includes such steps as extracting their active components, filtering by millipore membrane, and purifying by macroreticular resin. Said polyose product can be used for treating diabetes, hyperlipemia, tumor, etc and improving immunity.
US20110065762 Methods of use of antiviral compounds The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.
US20090163407 Compositions and methods for altering wnt autocrine signaling The present invention relates to compounds and methods for treating cancers in which the autocrine Wnt canonical signaling pathway is activated. In particular, there is provided a method for inhibiting growth of a tumor cell or sensitizing a cancer cell to treatment by contacting such a tumor cell with a compound that alters Wnt signaling. The compound that alters Wnt signaling can be a Wnt antagonist, a Wnt receptor antagonist, or a combination thereof.
EP2544688A2 Methods and compositions for treatment of angelman syndrome and autism spectrum disorders Methods for the treatment of Angelman Syndrome autism spectrum disorders are provided. The methods comprise administrating to a subject an agent that increases the expression of, or increases activity of, ?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) at neuronal synapses.
CN103751484A External medicinal liquor for treating fibromyalgia The invention discloses external medicinal liquor for treating fibromyalgia. The external medicinal liquor consists of myrrh, frankincense, drynaria rhizome, Chinese alangium root, dragon blood, aconite, monkshood, artemisia rupestris, borneol and 40-dgree pure rice wine. The medicinal liquor is prepared by naturally drying and crushing the medicinal materials, putting the medicinal materials in a container, immersing the medicinal materials in 40-degree pure rice wine, filtering and uniformly stirring with borneol. The external medicinal liquor can be used for treating arthritis, deadlimb, back pain, scapulohumeral periarthritis, cervical pain, rheumatoid, hyperostosis, sciatica, bruises and lumbar disc herniation, general pains can be eliminated when the external medicinal liquor is applied for 3-5 days, and patients with serious pains can be healed in 10-15 days. The external medicinal liquor has curative effect to mosquito bite, various skin itches and other diseases, does not have side effect, and is low in treatment cost.
WO2014055911A1 Bicyclic 1, 2, 4-oxadiazoles derivatives as sphingosine-1 phosphate receptors modulators The present invention relates to bicyclic aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
US20070254837 Treatment for Necrotizing Enterocolitis The invention provides compositions and methods for the treatment of necrotizing enterocolitis (NEC). A treatment of epidermal growth factor (EGF) receptor agonist and L-arginine, a bioequivalent thereof, or NO-donor showed efficacy against NEC. The invention also provides kits, unit doses and uses comprising epidermal growth factor (EGF) receptor agonist and L-arginine, a bioequivalent thereof, or NO-donor for the treatment of NEC.
CN103339128A Azaindoles as respiratory syncytial virus antiviral agents The invention relates to an azaindoles having inhibitory activity on RSV replication and having the formula (I) compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
EP1667641A1 Cosmetic or dermatological preparations having a content of isoflavones and licochalcone a The invention relates to preparations containing active substance combinations consisting of isoflavones and licochalcone A or of an aqueous extract from Radix Glycyrrhizae inflatae containing licochalcone A or to the use of active substance combinations consisting of isoflavones and licochalcone A or of an aqueous extract from Radix Glycyrrhizae inflatae containing licochalcone A for reducing the production of sebum.
CN103520633A Processing method of anticancer blood-circulation activating and mass disintegrating ointment The invention relates to the field of medicine, and in particular relates to a processing method of an anticancer blood-circulation activating and mass disintegrating ointment. The formula of 100 mass disintegrating pastes comprises the following components: 15-20g of short-pedicel aconite root, 15-25g of pyrolusite, 15-25g of Yunan panax notoginseng, 10-15g of unprocessed radix aconiti, 10-15g of raw kusnezoff monkshood root, 8-10g of angelica, 5-10g of chuanxiong rhizome, 8-10g of clematis root and 8-10g of safflower, which are weighed according to the formula, crushed by a machine and then processed into an ointment for external use. In combination with a transdermal therapy and a channels-collaterals therapy, the ointment is externally pasted on focuses and points to internally treat difficult miscellaneous diseases including tumor, rachitis, osteonecrosis and the like, and accords with the modern direction for safely and effectively treating tumor, rachitis and osteonecrosis. The processing method is scientific, advanced and practical.
CN102786493A 2,3-diaryl thiazolidinone compound and analogue, and purpose thereof in preparing antiangiogenic drugs The invention discloses a 2,3-diaryl thiazolidinone compound shown in a structural formula (I), a hydrate and pharmaceutically acceptable salts thereof, and a pharmaceutical composition containing the compound, as well as the application of the compound in preparing drugs capable of treating related diseases caused by all kinds of pathological angiogenesis.
CN101712672A Novel compound for treating diseases of cardiovascular and cerebrovascular systems, preparation method and application thereof The invention relates to the field of the chemistry of natural medicines, which discloses a compound extracted and separated from draconis sanguis and used for treating cardiovascular and cerebrovascular diseases. The constitutional formula of monomeric compound is as formula (1). The invention also relates to a preparation method of the compound and an application of the compound in the field of medicine, in particular to an application of the compound in the aspect of preparing a medicine for preventing and treating the cardiovascular and cerebrovascular diseases.
CN101703485A Ambroxol hydrochloride pill and preparation method thereof The invention relates to the technology of medicine, and discloses a preparation method of a pill by taking ambroxol hydrochloride as a component. The method comprises the steps: adding the ambroxol hydrochloride into molten base materials by adopting a molting and suspending assistant method, and a solid dispersing and mixed suspending technology and by means of mixed suspending dispersing and assistant suspending; stirring to be even mixed suspension liquid; and dipping into cooling liquid, and cooling to obtain the pill. The pill has high medicine content, fast disintegrating and dissolving, stable quality, small volume, can be orally taken or buccally taken, and is very suitable for old persons and bedridden patients who suffer from dysphagia.
WO2006085815A1 Thiazole derivatives, their process for their preparation and their use in therapy The invention provides compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein A, R1, R2 and R3 are as defined in the specification; a process for their preparation; pharmaceutical compositions containing them; and their use in therapy.
CN102846840A Preparation method of Tibetan medicine for treating acquired immune deficiency syndrome The invention discloses a preparation method of a Tibetan medicine for treating acquired immune deficiency syndrome. The Tibetan medicine comprises active components or the active components and pharmaceutically-acceptable auxiliary materials, wherein the active components are prepared by pure copper ash, semen hyoscyami paste, wood of shiny-leaved yellowhorn paste, Tibetan codonopsis pilosula, cortex berberidis, fructus podophylli and benzoin according to a certain weight ratio. The Tibetan medicine can be prepared into any one of common orally-taking drug forms. The Tibetan medicine has effects of clearing heat, removing toxicity, resolving hard lump, performing swelling subsidence and strengthening the body resistance. The Tibetan medicine mainly treats aeipathia, yellow water, the acquired immune deficiency syndrome, lymphopathy and eleven kinds of internal and external lumps in the abdomen referred by the Tibetan medicine. The Tibetan medicine considers that the root cause of all the aeipathia is indigestion, and digestion does not cause the aeipathia.
CN103550156A Preparation method of supermolecule globular micelle based on antidepressant medicament chlorpromazine The invention discloses a preparation method of a supermolecule globular micelle based on an antidepressant medicament chlorpromazine. The method comprises the following steps: constructing a medicament carrier through the supermolecule interaction of amphiphilic sulfonated calix [4] arene and an antidepressant medicament chlorpromazine hydrochloride, dissolving the amphiphilic sulfonated calix [4] arene and the antidepressant medicament chlorpromazine hydrochloride in water, and uniformly mixing to obtain a nano supermolecule globular micelle solution; and non-covalently modifying a targeting agent trimethyl chitosan through a bonding site of the calix arene on the surface of the micelle to obtain the supermolecule micelle loaded with trimethyl chitosan on the surface. The preparation method has the advantages that the preparation method is simple and convenient, and fewer subjective and objective raw materials are used; the medicament load rate is high since the medicament molecules are the constructing units of the medicament carrier and the medicament molecules are immobilized; the micelle can be used for non-covalently modifying the targeting agent trimethyl chitosan through the bonding site of the surface calix arene so that the micelle has a wide application prospect in the field of targeted medicament delivery.
US20060025434 Therapeutic agents for drug/substance dependence Therapeutic agents for drug/substance dependence containing a compound represented by the following compound: as an active ingredient. The therapeutic agents are excellent in the capability to penetrate into the brain, can promote the recovery from the state of psychological and physical dependent on dependence drugs/substances, can inhibit the craving and exacerbation, and are useful for treating drug/substance dependence and drug/substance dependence patients.
CN103690865A Nursing powder for spine surgery postoperative incision and preparation method thereof The invention discloses nursing powder for a spine surgery postoperative incision and a preparation method thereof and aims to solve the treatment problem that a patient feels discomfortable due to the postoperative incision. The preparation method is characterized by comprising the steps: (1) extracting volatile oil from semen aesculi, ivy glorybind herb roots, jasminum grandiflorum, loose knots and lychee seeds for later use; (2) grinding hard sinapis semina paste powder, magnetites and puerarin into fine powder for later use; (3) performing water extraction and alcohol sedimentation on roots of Sandhill Tylophora, platycodon grandiflorum, alpinia japonica and asterina pectinifera, and drying the materials to obtain initial materials; (4) spraying the volatile oil into the initial materials, adding the fine puerarin powder, uniformly stirring, screening through a sieve of 60 meshes, and packaging and applying to obtain the nursing powder. The clinical experiment shows that the nursing powder has the characteristics of good treating effect on the discomfort of the postoperative incision and higher safety and deserves to be clinically applied and popularized.
US8067385 Antiviral oligonucleotides targeting HBV Random sequence oligonucleotides that have antiviral activity are described, along with their use as antiviral agents. In many cases, the oligonucleotides are greater than 40 nucleotides in length. Also described are methods for the prophylaxis or treatment of a viral infection in a human or animal, and a method for the prophylaxis treatment of cancer caused by oncoviruses in a human or animal. The methods typically involve administering to a human or animal in need of such treatment, a pharmacologically acceptable, therapeutically effective amount of at least oligonucleotide that does not act by a sequence complementary mode of action.
CN103656627A Vitamin C collagen compound effervescent tablet and preparation method thereof The invention relates to a vitamin C collagen compound effervescent tablet and a preparation method thereof. The vitamin C collagen compound effervescent tablet comprises the following components in weight percentage: 0.5-2% of vitamin C, 25-40% of collagen, 5-15% of phycocyanin, 5-15% of whey protein, 5-15% of inulin, 1-5% of green tea extract and 5-10% of grape seed extract which are used as main raw materials, and 5-10% of sodium bicarbonate, 5-10% of tartaric acid, 2-5% of citric acid, 2-5% of povidone, 5-10% of stevia sugar and 0.5-2% of magnesium stearate which are used as auxiliary materials. The vitamin C collagen compound effervescent tablet is natural in component, scientific in proportion, convenient to carry and take, safe and reliable, has a rapid effect after dissolution, resists aging and has a remarkable effect of maintaining beauty and keeping young; the preparation method is reasonable in process, the operability is high, and the large-scale production is easy to realize.
US20080292579 Polymer-Based Serum Albumin Substitute This invention provides the use of a polymer comprising a hyperbranched polyether polyol such as hyperbranched polyglycerol as a serum albumin substitute. Also provided are high molecular weight hyperbranched polyglycerol polymers suitable for a variety of medical and non-medical uses including methods for making such high molecular weight polymers.
US7854717 uses ultrapheresis, refined to remove compounds of less than 120,000 daltons molecular weight, followed by administration of replacement fluid, to stimulate the patient's immune system to attack solid tumors A method to treat cancer uses ultrapheresis, refined to remove compounds of less than 120,000 daltons molecular weight, followed by administration of replacement fluid, to stimulate the patient's immune system to attack solid tumors. In the preferred embodiment, the patient is ultrapheresed using a capillary tube ultrafilter having a pore size of 0.02 to 0.05 microns, with a molecular weight cutoff of 120,000 daltons, sufficient to filter one blood volume. The preferred replacement fluid is ultrapheresed normal plasma. The patient is preferably treated daily for three weeks, diagnostic tests conducted to verify that there has been shrinkage of the tumors, then the treatment regime is repeated. The treatment is preferably combined with an alternative therapy, for example, treatment with an anti-angiogenic compound, one or more cytokines such as TNF, gamma interferon, or IL-2, or a procoagulant compound. The treatment increases endogenous, local levels of cytokines, such as TNF. This provides a basis for an improved effect when combined with any treatment that enhances cytokine activity against the tumors, for example, treatments using alkylating agents, doxyrubicin, carboplatinum, cistplatimum, and taxol. Alternatively, the ultrapheresis treatment can be combined with local chemotherapy, systemic chemotherapy, and/or radiation.
EP1659115A1 Synthesis of substituted 2H-indazole derivatives as anti-angiogenic agents Novel compounds of 2-(substituted arylmethyl)-3-(substituted phenyl)-2H-indazoles and 1-(substituted arylmethyl)-3-(substituted phenyl)-1H-indazoles are synthesized, and useful as anti-angiogenic agents.
US7262044 Sphingosine-1-phosphate lyase polypeptides, polynucleotides and modulating agents and methods of use therefor Compositions, methods and kits for diagnosing and treating cancer are provided. Therapeutic compositions may comprise agents that modulate the expression or activity of a sphingosine-1-phosphate lyase (SPL). Such compositions may be administered to a mammal afflicted with cancer. Diagnostic methods and kits may employ an agent suitable for detecting alterations in endogenous SPL. Such methods and kits may be used to detect the presence of a cancer or to evaluate the prognosis of a known disease. SPL polypeptides, polynucleotides and antibodies are also provided.
CN101549152A Alliin/alliinase dualistic drug-releasing multilayer tablet that can resist infection diseases caused by helicobacter pylori and candida albicans and the like The invention discloses a method for preparing an alliin/alliinase dualistic drug-releasing multilayer tablet that can resist infection diseases caused by helicobacter pylori and candida albicans and on the like. The tablet is composed of three layers, namely, an alliin layer, a separation layer and an alliinase layer. The outside of the tablet is wrapped by an intestine-dissolving film coat (for oral administration) or a common film coat (for vagina application). When the tablet is swallowed, the intestine-dissolving film coat (for oral administration) or the common film coat (for vagina application) is dissolved by body fluid, and the alliin and the alliinase meet each other and generate catalysis effect to produce allicin, thus having the drug effect of anribacterium to pathogenic bacterium such as the helicobacter pylori and candida albicans and the like.
US20110066117 Large volume enema An enema comprises a bottle, and at least 150 ml of a solution in the bottle. The solution comprises water, 5.00 to 8.00 grams dibasic sodium phosphate, and 15.00 to 21.00 grams monobasic sodium phosphate.
CN102370635A Application and preparation method of novel nardosinone The invention discloses application and a preparation method of novel nardosinone. The preparation method comprises the following steps of: refrigerating a nard medicinal material, smashing, screening with a screen of 20-60 meshes, adding ethanol of which the amount is 8-12 times that of the nard medicinal material, soaking, and performing percolation extracting for 1-3 times, every time for 12-36 hours; and recovering ethanol under reduced pressure, concentrating till ethanol smell disappears, adding ethyl acetate for dissolving, stirring with coarse silica gel, separating with a silica gel column of 200-300 meshes, and gradually eluting with petroleum ether and ethyl acetate in the ratio 10:0 and with petroleum ether and ethyl acetate in the ratio 9:1 to obtain novel nardosinone.
US7217730 Method for the use of pyranoindole derivatives to treat infection with Hepatitis C virus The invention is directed to methods of treating, preventing, or inhibiting a Hepatitis C viral infection in a mammal comprising contacting the mammal with an effective amount of a compound of the formula: Wherein substitutions at R1, R2, R3—R12, and Y are set forth in the specification.
US20120093928 Oral metaxalone compositions The present invention relates to a pharmaceutical composition comprising low-dose metaxalone and one or more pharmaceutically acceptable polymer, as well as methods of preparing them.
CN103222986A Application of gingerol and ruddle composition in preparation of attenuated synergistic medicaments in cancer chemotherapy The invention relates to a medicine composition, a preparation method and an application of the medicine composition in preparation of attenuated synergistic medicaments in cancer chemotherapy, the natural medicine composition is composed of gingerol and ruddle according to ratio of 3-9:1, the composition has good curative effect for vomiting side effects due to cancer chemotherapy, and has the effect for inhibiting tumor.
US20100204217 Treatment for leukemia and idiopathic aplastic anemia A process for treating a patient with leukemia or an aplastic anemia having cells with inclusions that stain with anti-E. canis antibodies or antibodies to other Ehrlichia or Anaplasma is disclosed. That process comprises administering to the patient (i) an antibacterial amount of a rifamycin, (ii) an antibacterial amount of a quinolone, or a mixture of (i) and (ii).
CA2264929C Semi-synthetic sulphaminoheparosansulphates having high anti-metastatic activity and reduced haemorrhagic risk Sulphaminoheparosansulphates obtainable from the Escherichia coli K5 polysaccharide by deacetilation and the subsequent sulfation with the sulphuric anhydride/trimethylamine adduct carried out at 0°C, for times ranging from 0.25 to 2 hours and using a reactant/polysaccharide ratio (SO3 equivalents/available OH groups equivalents) equal to 5 have been found having high anti-metastatic activity and low anticoagulant activity.
EP1603575A2 Nemorubicin as radiosensitizer in combination with radiation therapy against tumors The present invention relates to a morpholinyl anthracycline derivative for use as radiosensitizer, to be administered in combination with radiation therapy, so that a synergistic effect can be revealed.
EP1539141B1 3-(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, and Y are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
US20050207976 High energy phototherapeutic agents A high energy phototherapeutic agents or radiosensitizer agent comprised of a halogenated xanthene, or an agent that exhibits a preference for concentration in biologically sensitive structures in diseased tissue, and methods of treating and imaging using radiosensitizer agents in diseased tissue.
US20100113501 Ophthalmic Composition Comprising Ascomycin This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis.
CN103330707A Cimetidine composition for injection The invention provides a cimetidine composition for injection, and relates to the technical field of medicines and medicine manufacturing. Main medicines of the composition are cimetidine and melatonin. The melatonin comprises a quick release part and a slow release part contained in cyclodextrin. The cimetidine composition for injection provided by the invention has the functions of improving the treatment effect on upper gastrointestinal hemorrhage, shortening the course of treatment, further reducing the use level of cimetidine and lowering the side effect of cimetidine. Instability, fast distribution and elimination and the like of MT (Melatonin) caused by oral absorption are avoided, and the first pass effect of MT is reduced. Delivery design combining quick release and slow release meets the secretion characteristic of MT, solves the problem of short half life of MT and improves the bioavailability of the product.
CN101284085A Plaster for curing the bone fracture The invention discloses a plaster for treating bone wound. The plaster contains vegetable oil 3-10 weight parts, rosin 30-60 weight parts, formic acid or acetic acid 4-6 weight parts, camphor 3-5 weight parts, calomel 4-8 weight parts, mercuric oxide 6-10 weight parts, dragon's blood 10-15 weight parts, borneol 6-12 weight parts, myrrh 10-14 weight parts, white alum 6-10 weight parts, and rhubarb 4-8 weight parts. The plaster has the advantages of large drug carrying capacity and high water content and permeation and can be used for treating general fracture, bone degeneration and damage, joint degeneration, periostitis, traumatic arthritis, periarthritis humeroscapularis, rheumatic arthritis, etc.
WO2010130424A1 1,2,3-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 ("mGluR2"), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
US7928124 N-aroyl cyclic amine derivatives as orexin receptor antagonists Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.
EP1140017B1 Water-insoluble drug delivery system The present invention provides a drug delivery system comprising a water-insoluble drug, a water-miscible organic solvent for the water-insoluble drug, a surfactant, and water, as well as a process for preparing the same. This invention further provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and such a drug delivery system. In addition, the present invention provides a method of delivering a drug to a host by administering to the host the drug delivery system of the present invention.
CN101590066A Medicinal application of 1,6-diphosphate fructose in treating epilepsy complication and preventing epilepsy The invention discloses application of 1,6-diphosphate fructose, prodrug thereof or pharmaceutically acceptable salt thereof in preparing a medicament for preventing epilepsy, a medicament for radically treating epilepsy, a medicament for treating epilepsy complication or a medicament for improving the treatment effect of the prior medicament for resisting epilepsy, wherein the pharmaceutically acceptable salt of the 1,6-diphosphate fructose comprises sodium salt, potassium salt, calcium salt, magnesium salt, manganese salt, ammonium salt or amine salt. The medicament contains treatment effective quantity of the 1,6-diphosphate fructose, the prodrug thereof or the pharmaceutically acceptable salt thereof, and pharmaceutically acceptable excipient or carrier, and also can contain other compounds for resisting the epilepsy. The medicament can be tablets, oral liquid, pill, dripping pills, capsules, granules, oral slow-release preparation, oral controlled-release preparation, targeting preparation, injection, powder, infusion solution or suppository.
US20120295956 Prevention of tissue ischemia and related methods Provided herein are methods for preventing, ameliorating, and/or reducing tissue ischemia and/or tissue damage due to ischemia, increasing blood vessel diameter, blood flow and tissue perfusion in the presence of vascular disease including peripheral vascular disease, atherosclerotic vascular disease, coronary artery disease, stroke and influencing other conditions, by suppressing CD47 and/or blocking TSP1 and/or CD47 activity or interaction. Influencing the interaction of CD47-TSP1 in blood vessels allows for control of blood vessel diameter and blood flow, and permits modification of blood pressure and cardiac function. Under conditions of decreased blood flow, for instance through injury or atherosclerosis, blocking TSP1-CD47 interaction allows blood vessels to dilate and increases blood flow, tissue perfusion and tissue survival.
WO2007003308A1 Substituted quinolones ii The invention relates to substituted quinolones of formula (I) and to a method for the production thereof as well as to the use thereof in the manufacture of medicaments for the treatment and/or prophylaxis of diseases, more particularly the use thereof as an antiviral agent, in particular against cytomegalo viruses.
EP1100763B1 Diketoacid-derivatives as inhibitors of polymerases Diketoacids of Formula (A) are useful as inhibitors of viral polymerases. In particular hepatitis C virus RNA dependent RNA polymerase (HCV RdRp), hepatitis B virus polymerase (HBV pol) and reverse transcriptase of human immunodeficiency virus (HIV RT). The group R may be broadly chosen and is an organic moiety which contains 2 to 24 carbon atoms and includes an optionally cyclic or heterocyclic group in which the atom directly bonded to the adjacent carbonyl in the diketoacid is part of the ring structure.
CN1839863A Diabetes-treating pharmaceutical compositions and its preparing method and uses The invention discloses a pharmaceutical composition for treating diabetes, which comprises trigonella foenum graecum saponin as the active portion, and pharmaceutically acceptable adjuvant or supplementary constituents, wherein the trigonella foenum graecum saponin is the extract of Trigonella foenum-graecum L., the content of the trigonella foenum graecum saponin is greater than 65% calculated by weight percent of trigonella foenum graecum saponin B. The effective ingredients of trigonella foenum graecum saponin A, B, C and D are determined in the specification.
CN1989928A Speckle dispelling agent The invention relates to a medicament for eliminating flecks whose main compositions include ascorbic acid, hydroquinone, sodium acid sulfite, citric acid, sodium dodecylsulfate, stearyl alcohol, glyceryl monostearate, stearic acid, glycerin, titanium oxide, perfume compounds and distilled water. The medicament is prepared through specific processes.
US20050131043 Phenylethynyl and styryl derivatives of imidazole and fused ring heterocycles This invention relates to a compound and the use of the compound of the formula wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies —CH═CH— or —C≡C—; and B signifies wherein R6 to R26, X and Y are as defined in the specification or a pharmaceutically acceptable salt thereof, for use in pharmaceutical compositions for the treatment or prevention of mGluR5 receptor mediated disorders.
CN103393595A Pharmaceutical composition of edaravone The invention belongs to the technical field of medicines, and discloses a pharmaceutical composition of edaravone, and in particular relates to the pharmaceutical composition containing edaravone, sodium chloride, organic acids and L-cysteine hydrochloride monohydrate. Stability researches indicate that a transfusion preparations prepared from the pharmaceutical composition has better stability and more excellent quality.
CN102000061A Medicinal application of nitrobenzoyl silybin to preparation of glycosidase inhibitor The invention relates to medicinal application of nitrobenzoyl silybin to preparation of a glycosidase inhibitor, and in particular discloses silybin ester type flavone lignan substituted by a nitrobenzoyl group and application of a pharmaceutically acceptable salt thereof to preparation of medicaments for inhibiting alpha-glucosidase and preventing II-type diabetes. The flavone lignan has extremely obvious activity of suppressing the alpha-glucosidase; and the measurement of the median inhibitory concentration shows that the strength of the flavone lignan for inhibiting the alpha-glucosidaseis 34 times that of acarbose serving as a positive contrast medicament. The pharmacodynamic result shows that the flavone lignan or the pharmaceutically acceptable salt thereof can be expected to be used as a glucosidase inhibitor medicament, particularly a medicament for preventing the II-type diabetes, namely non-insulin dependent diabetes.
WO2008024765B1 Therapeutic substituted thiazolidinones, oxazolidinones, and related compounds A compound having a structure (I) or (II) is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
CN1864693A A glycerin and fructose injection and preparation method thereof The present invention relates to one kind of glycerine-fructose injection and its preparation process. The injection in 250 liters consists of glycerine fructose in 25 kg, fructose in 12.5 kg, sodium chloride in 2.25 kg and water for injection for the rest, and may be compounded into 1000 bottles of transfused solution of 250 ml each or 500 bottles of transfused solution of 500 ml each. The present invention also provides the preparation process of the injection.
CN1876152B A medicine for treating nervous deafness and preparation process thereof The invention relates to a medicament for treating nerve deafness and process for preparation, wherein the medicament is prepared from epimeddium, fleece-flower root, prepared rehmannia root, Siberian solomonseal rhizome, tortoise shell, magnetite, Ligusticum wallichii, curcuma aromatica, astragalus root and batryticated silkworm through the steps of grilling, filtering, mixing, ethanol extracting, mixing filtrate, concentrating, drying and making capsules.
WO2013051159A1 Nop receptor antagonist A novel excellent non-opioid branch of the opioid peptide family of receptors antagonist is provided, which exhibit an analgesic effect on a varuous pains. The present invention is directed to a non-opioid branch of the opioid peptide family of receptors antagonist represented by the general formula [1] or a pharmaceutically acceptable salt thereof. In the general formula [1], R1 represents hydrogen or the like, R2 represents hydrogen or the like, R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen, R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy, R6 represents (1) alkyl, (2) cycloalkyl, (3) phenyl, (4) a 5- to 10-membered aromatic heterocyclic group containing 1 to 3 heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or (5) -N(R61)(R62).
US7276532 Incontinence The present invention provides a therapeutic agent for overactive bladder comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like; X1—X2—X3 represents CR5═CR6—CR7═CR8, CR5═CR6—S, and the like; Y represents —CH2S—, —SOCH2—, and the like; and R2 represents a hydrogen atom, and the like] or a pharmaceutically acceptable salt thereof.
US20110009495 Inhibition of the Survival of Bone Cancer by Cyclohexenone Compounds from Antrodia Camphorata The present invention relates to a novel application of a compound. The compound 4-hydroxy-2,3-dimethoxy-6-methyl-5-(3,7,11-trimethyl-dodeca-2,6,10-trienyl)-cyclohex-2-enone of the invention is isolated and purified from the extracts of Antrodia camphorata, which can be applied for inhibiting the survival of bone cancer cells and be used as a pharmaceutical composition to inhibit the bone tumor growth.
EP1638936A1 3-oxa-8-azaprostaglandin analogs as agents for lowering intraocular pressure The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula (I); wherein X, Y, Z, d and R3 are as defined in the specification.
CN203389118U Health-care ball capable of sterilization and magnet therapy The utility model discloses a health-care ball capable of sterilization and magnet therapy. The health-care ball comprises an ellipsoidal metal ball body, wherein a containing cavity is formed in the metal ball body; the metal ball body comprises an upper metal ball shell and a lower metal ball shell which are distributed symmetrically and are ellipsoidal; the upper metal ball shell is buckled with the lower metal ball shell; the containing cavity is commonly enclosed by the upper metal ball shell and the lower metal ball shell; a silver paste layer is uniformly coated on the outer surface of the metal ball body; magnets are filled in the containing cavity of the metal ball body. The metal ball body adopts a splitting type structural design so that the machining and the assembling are convenient and the preparation cost is low; the metal ball body with the ellipsoidal structure design can keep the large contact area with the skin; in the working process, silver ions of the silver paste layer can kill bacteria; the magnets in the containing cavity release a magnetic field which can act on corresponding parts of a human body so as to realize the effects of the magnet therapy. Therefore, the health-care ball can simultaneously realize sterilization and magnet therapy functions and has the advantages of various functions and convenience for utilization.
CN101575318A Novel dihydropyridine compound and application thereof on preparing drugs for curing and/or preventing virus diseases The invention relates to novel dihydropyridine compound and application thereof on preparing drugs for curing and/or preventing virus diseases, in particular to a compound shown as general formula (1) and isomers, salts for medicinal purpose or hydrate thereof, and each variable is defined as in a specification. The invention also relates to a preparing method of compound shown as general formula (1), and an application of a compound shown as general formula (1) and isomers, salts for medicinal purpose or hydrate thereof, in particular to application in preparing drugs for curing and/or preventing hepatitis B.
EP1536782A1 Synergistic combination of an alpha-2-delta ligand and a pdev inhibitor for use in the treatment of pain The instant invention relates to a combination of an alpha-2-delta ligand and a PDEV inhibitor for use in therapy, particularly in the curative, prophylactic or palliative treatment of pain, particularly neuropathic pain. Particularly preferred alpha-2-delta ligands are gabapentin and pregabalin. Particularly preferred PDEV inhibitors are sildenafil, vardenafil and tadalafil.
CN102441118A Application of medicinal composition in preparing medicaments for treating diabetes mellitus and impaired glucose tolerance The invention relates to novel application of a medicinal composition in preparing medicaments for treating diabetes mellitus and impaired clucose tolerance. The medicinal composition comprises 480 parts of axillary choerospondias fruit, 240 parts of red-rooted salvia root, 60 parts of clove, 30 parts of borneol, and 30 parts of tabasheer. The medicinal composition can be pills, granules, hard capsules, soft capsules, tablets, dripping pills or oral liquid. The invention aims at providing novel treatment application of the medicinal composition, so that the clinical application range of the medicinal composition provided by the invention is enlarged, and waste of excellent medicinal resources is avoided.
CN103570692A Quinazoline derivative with ethylene imine ring side chain as well as preparation and application The invention discloses a quinazoline derivative which contains an ethylene imine ring side chain and is as shown in formula I in the specification, or an enantiomer of the derivative. A target compound is prepared mainly by carrying out one-step condensing on 4-arylamine quinazoline as a nuclear parent and ethylene imine formic acid, and modifying later. Tests show that the quinazoline derivative has a remarkable anti-proliferative effect on tumor cells associated with EGFR (Epidermal Growth Factor Receptor) tyrosine kinase activity in cellular level, such as human epidermoid carcinoma cell strain A431 over-expressing EGFR and Gefitinib-resistant human lung adenocarcinoma cell strain H1975, particularly has a good inhibition effect on the drug-resistant cell strain H1975, and meanwhile has a good inhibition effect on EGFR kinase, so that the quinazoline derivative can be prepared into corresponding anti-tumor cell medicaments.
CN101768124A Medicine crystal, preparation method and purpose thereof The invention discloses a new rufinamide crystal and a preparation method thereof. An infrared spectrum is determined by an X-ray powder map method and a KBr sheeting-transmission method, and thermal analysis determination is carried out by a differential scanning magnitude method. A preparation prepared by the new crystal has good dissolution degree and is more suitable for being used by a patient suffering from epilepsy at the stage of attack.
WO2010086278A1 Novel benzodioxolyl-oxadiazolyl-diazabicyclononane derivatives and their medical use This invention relates to novel benzodioxolyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances (I).
CN103315106A Making method of bagged tea for reducing blood pressure and blood fat The invention relates to making method of bagged tea for reducing blood pressure and blood fat. The bagged tea is made by the following raw materials in parts by weight: 600-900 parts of folium cortex eucommiae and 100-400 parts of roadleaf holly leaves. The making method comprises the following steps of: performing reflux extraction on folium cortex eucommiae by an ethanol liquor, and concentrating the filtrate to cream for later use; crushing 50-70wt% of roadleaf holly leaves to coarse powder, adding water to soak the rest of roadleaf holly leaves, adding Eucommia ulmoides residue, combining and decocting, filtering, filtering and concentrating to cream, adding an Eucommia ulmoides alcohol extract and mogroside, and after adequately and uniformly mixing and blasting into dried rest roadleaf holly leave coarse powder; and finally, sterilizing the target product at high temperature in short time, and drying and neatening at low temperature, and packaging. The bagged tea obtained by the making method has the characteristics of meticulous and uniform particles, high content of medicinal components, uniform distribution, quick dissolving-out speed and the like, and the bag tea is slightly sweet in taste, faint scent and mellow in flavor, and meanwhile, the bag tea enhances the treatment effect on hypertension and hyperlipidemia, and further improves the medicinal additional value of blood sugar reducing medicines and the like. The bag tea is another optimal choice for patients with hypertension, hyperlipidemia and hyperglycemia.
US20110135580 Novel Medicament Combinations for the Treatment of Respiratory Diseases The present invention relates to new medicament combinations which contain in addition to one or more, preferably one, compound of general formula 1 wherein the groups A, B, X, R1, R2 and R3 may have the meanings given in the claims and specification, at least one anticholinergic 2 and at least one steroid 3, processes for preparing them and their use as pharmaceutical compositions.
WO2014093918A1 Compositions and methods comprising polyethylene glycol and magnesium for treatment of neuronal injury The disclosure provides compositions, methods and kits for treatment of neuronal injury. In one embodiment, the composition comprises polyethylene glycol (PEG), and magnesium in one composition. In another embodiment, the composition comprises PEG, and magnesium, where the PEG is in separate composition and the magnesium is in a separate composition. In yet another embodiment, the PEG and/or the magnesium may be administered to treat spinal cord injury.
EP2638903A1 Suppressor for increase in blood glucose level The present invention relates to an agent for inhibiting elevation in postprandial blood glucose level, which comprises an ester of EPA or DHA ester as an active ingredient, and which is to be administered between meals. The invention provides an agent for inhibiting elevation in blood glucose level that has a high level of safety and desirable characteristics such as storage stability, in particular, a means for reducing postprandial hyperglycemia.
WO2007088196A1 Use of alkylglucoside esters as beta-defensin inducers The present invention relates to the use of alkylglucoside esters for the manufacture of a dermatological or dermocosmetological topical composition for use in the preventive or curative treatment of microbial conditions through the induction of the expression of endogenous antimicrobial peptides.
EP0793499B1 Method and composition for reducing tumor development with a combination of a taxane compound and a tellurium and/or selenium compound There are provided compositions for, and a method of, treating malignancies which comprise effective amounts of a novel combined therapy comprising a taxane compound, e.g., paclitaxel, and a tellurium or selenium compound, e.g., ammonium trichloro(dioxoethylene-O,O-tellurate), and administering the respective compounds simultaneously or separately.
WO2014154117A1 Isothiocyanate, preparation method therefor, and use against cancer An isothiocyanate having the following structural formula (I). The isothiocyanate synthesis processing technique is as follows: obtained by using conventional organic bases, carbon disulfide, and acetyl chloride to react in a low temperature or room temperature environment. The isothiocyanate has substantial damaging effect on tumor cells.
US20120289510 Benzyl Amines, A Process For Their Production And Their Use As Anti-Inflammtory Agents The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.
CN103083449A Stop-bleeding medicine and preparation method thereof The invention belongs to the technical field of stop-bleeding medicine, and particularly relates to a stop-bleeding medicine and a preparation method thereof. The stop-bleeding medicine is prepared from the following raw materials in parts by weight: 15 parts of golden cypress, 40 parts of puffball, 70 parts of loofah flower and 2 parts of borneol. The preparation method comprises the steps of: grinding the raw materials into fine powder; and filling the raw materials in a bottle for standby application. The stop-bleeding medicine disclosed by the invention has a simple formulation, is convenient, effective, economic and portable, and can be easily taken by a patient; and the stop-bleeding medicine can stop pain, diminish inflammation and stop bleeding, and has remarkable effects.
WO2009097278A1 6-SUBSTITUTED-THIO-2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) The present invention is directed to 6-substituted-thio-2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and / or dementia. The compounds of the present invention are inhibitors of β- secretase, also known as β-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2.
EP2227453A2 Heteroaryl amides useful as inhibitors of voltage-gated sodium channels The present invention relates to compounds of formula I'' useful as inhibitors of voltage -gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
CN101502508A Application of 5-oxo-4-alkenylene-pyrazole derivative in preparing anti-tumor medicament The invention belongs to the field of genetic engineering and chemistry and relates to the application of 5-oxo-4-alkenylene-pyrazole derivatives in the preparation of anti-tumor drugs. The biomedical field is focused on finding novel anti-tumor drugs with low side effects, therefore, the invention provides the application of 2-{2-bromo-6-methoxy-4-[(Z)-(5-oxo-1,3-diphenyl-1,5-dihydro-4H-pyrazol-4-ylidene)methyl]phenoxy}acetamide, a small-molecule compound, in preparing the anti-tumor drugs. The compound can obviously inhibit the proliferation of tumor cells and slow down the growth rate of mouse tumors, moreover, the compound, which is designed for the CYPJ protein structure of cellular targets, has particularly obvious effect on the tumor cells of highly-expressed CYPJ protein, therefore, by developing the small-molecule compound as a novel anti-tumor drug, the invention has obvious anti-tumor effect, reduces the damage on normal cells and ensures the good specificity.
WO2013021337A1 Antiviral compounds with a fused tricyclic ring Compounds of the general formula I, their tautomeric forms, their stereoisomers, their analogs, their prodrugs, their isotopes, their N-oxides, their metabolites, their pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as antiviral candidate, more specifically as anti-HCV are disclosed.
CN102600198A Application of tebivudine compound in preparation of information therapeutic medicament, preparation method of tebivudine compound and new medicament prepared by utilizing tebivudine compound The invention discloses an application of tebivudine compound in preparation of an information therapeutic medicament, a preparation method of the tebivudine compound and a new medicament prepared by utilizing the tebivudine compound. The information therapeutic medicament is not directly contacted with a human body during therapy, no chemical composition of the medicament is consumed, a chemical therapeutic effect can be achieved by utilizing medicament information physical therapy only, the therapeutic window of the medicament is expanded by more than a thousand folds, and the side effect of chemotherapy is avoided. After tebivudine is used as the information therapeutic medicament, the content of active ingredients is not changed, and the tebivudine also can be used as a chemotherapy conventional preparation to be effectively used for a second time.
US20120225117 Process for production of w/o/w emulsion, process for production of liposome employing the process, and porous membrane for use in the processes The present invention provides a liposome production process which enables production of a liposome that has a nano-size particle diameter and a high water-soluble drug encapsulation rate. The process for producing a W1/O/W2 emulsion of the present invention includes the steps of (1) emulsifying an organic solvent (O) that is a volatile organic solvent, an aqueous solvent (W1) and a mixed lipid component (F1) to give a W1/O emulsion; and (2) dispersing the W1/O emulsion produced in step (1) in an aqueous solvent (W2) by use of a porous membrane, to give a W1/O/W2 emulsion, wherein the porous membrane has been surface-treated with a hydrophilic drug so as to allow its surface to have a water contact angle of 0 to 42° in the air.
CN101352445A Novel use of chuanbeinone compounds The invention discloses the new usage of proteimines compound. Being shown in formula (I) and formula (II), the new usage of the proteimines compound or the salt accepted by the proteimines compound in the pharmacology includes in the application of preparing the medicine for inhibiting eukaryote tumour cell proliferation and preparing and preventing and/or treating tumour. By combining the new usage of the proteimines compound or the salt accepted by the proteimines compound in the pharmacology which is shown in formula (I) and formula (II) and G-four strobila DNA, and the stability of the G-four strobila is enhanced, thereby competitive inhibition telomerase is combined with telomere, the activity of the telomerase is inhibited, the multiplication capacity of the cell is reduced, the extension of the telomerase is inhibited, and cell apoptosis is promoted. The proteimines compound or the salt accepted by the proteimines compound in the pharmacology which is shown in formula (I) and formula (II) has important significance in preparation of preventing and/or treating cancer.
CN101544952B Oxytropis ehrig cinerea FEL4-OOc and separation method and application thereof The invention discloses an oxytropis ehrig fungus alternaria FEL4-OOc which is preserved in the China type culture collection center on October 8, 2008, and the preservation code is CCTCC NO: M 208143. Bacterial colony of bacterial strain is in a circular shape with regular edges, the bacterial colony is white during early culturing period and gradually changes to gray, celadon and black as the culturing time is prolonged, and the centre of the bacterial colony slightly protrudes. Mycelium has transverse septa but has no mediastinums, and is relatively dense. Conidiophores peduncles grow on Part of the aging hypha, and the conidiophores peduncles have braches. The conidiophores are less in amount and brown in color, and are singly distributed in a scattered mode. The conidiophores have the2-5 transverse septa with thicker transverse septa films but have no mediastinums, ; spores are in long rod shapes and column shapes with the size of 30 to 90 microns*5 to 10 microns. The bacterial strain is obtained from leaves, stems, flowers or seeds of yellowflower crazyweed herbs through manual separation and filtration, and has the function of synthesizing main toxin, i.e. spherosin of the yellowflower crazyweed herbs.
WO2010149170A1 Treatment of insulin resistance and obesity by stimulating glp-1 release The present invention relates to 1 or 2 C16-C18 acyl glycerol based compounds which are capable of activating G-protein coupled receptor 119 and thereby stimulate GLP-1 release. Compounds of the present invention are useful in the prophylaxis and/or treatment of metabolic disorders and complications thereof, such as, type 2 diabetes mellitus (T2DM), obesity, insulin resistance, and cardiovascular disease.
CN101200426A Hydroxyl benzoic anhydride dimer compound, preparation method and uses thereof The present invention discloses symmetric and asymmetric m-hydroxybenzoic acid dimer compounds with constitutional formula (I), and as well as a method of the preparation of and the function of such products. Basic framework m-hydroxybenzoic acid and as well as hydroxybenzoic acid replaced by the same or different hydroxyl groups are condensed into m-hydroxybenzoic acid dimer compound with a parent nucleus symmetric structure and with the replacement of the same or different number of hydroxyl groups, the pharmacological test proves that the product has the activities of anti-human papillomavirus, herpes virus and resist HIV-1 integrase inhibitors; the product is capable to resist the virus that can integrally enter the chromosome of human cell, inhibit the breeding of the virus that integrally enter into the chromosome, prevent the relapse of virus infection; in addition, the product has antitumor activity.
WO2007104907A1 Improved formulation of comt inhibitors The present invention relates to an improved formulation of a COMT inhibitor, a process for its preparation and a pharmaceutical composition comprising the same. Further, it relates to such a composition for use in therapy, and the use of such a composition for the manufacture of a medicament for use in the treatment of Parkinson's disease.
WO2009128058A1 Psycho-pharmaceuticals The invention provides a compound for use in the treatment of symptoms associated with psychosis, schizophrenia, a cognitive impairment disorder, a mood disorder, a nervous system disorder and/or a behavioral disorder. The compound has the formula ? and is administered to a subject in need thereof in an effective amount. The compound Meparfynol (3-methylpent-l-yn-3-ol) has been found to be effective.
CN101152442A Preparations capable of effectively improving eyeground lesion and retina microcirculation lesion, and method for preparing the same A preparation which can effectively improve eyeground pathological change and pathological change of retina microcirculation and the preparation method relate to a preparation which can effectively improve eyeground pathological change and pathological change of retina microcirculation and the preparation method. The preparation is confected with prexeronine, docosahexenoic acid, eicosapentaenoic acid, mother of pearl, abalone shell, gynura segetum flower, antelope horn, turtle plastron, snake slough, chushizi, kapur, jiangcao, gentian, privet, raspberry, lutein, centipeda minima, polygonatum arisanense, Chinese atractylodes and belvedere fruit. The preparation method is that the abalone shell, purple tooth shell, turtle plastron and antelope horn are ground to powder and the gynura segetum flower, cicada flower, medlar, polygonatum arisanense, Chinese atractylodes and belvedere fruit are dried, crushed and sieved; and then the prexeronine, docosahexenoic acid, eicosapentaenoic acid are mixed, distilled and the auxiliary materials are added to make the preparation. The present invention adopts purified black pearl, fatsoluble retinol, amber and epimedium herb which have the function of promoting vision to make and can effectively improve the eyeground pathological change and pathological change of retina microcirculation.
CN1796380A Antibacterial compound A-28, and application in preparing antibacterial drug This invention publishes an antibacterial compound A-28 with a common formula (I), its application in manufacturing antibacterial drugs and its blended composite drugs. This compound, with its pharmacologically permitted ester derivatives, ether derivatives, amino-formyl-N-alkyl derivatives and salts, performs outstanding and broad-spectrum antibacterial activity. It is especially germicidal to leptospiras and some other G- or G+ bacteria and is thus applicable in curing or preventing infection diseases.
CN101422437A Etoposide dry suspension and preparation method thereof The invention relates to the technical field of medicament and discloses an etoposide dry suspension agent and a preparation method thereof. The suspension agent can quickly sputter and disperse to form uniform suspension liquid when being put in water, and is characterized by convenient use and high bioavailability; the preparation method, the production condition and the production technique of the suspension liquid are simple; and the use method thereof is more flexible, thus leading the old sufferers and the sufferers who have difficulty in swallowing to take the medicament conveniently, improving the dissolving rate and fully exerting the effect of the etoposide to cure solid tumors. The invention adopts the technical proposal as follows: the invention is a dry suspension agent which is prepared by taking the etoposide or the pharmaceutically acceptable salt thereof as an active component and taking a loading agent, a sorbent, a glidant, a suspension agent and/or a suspending aid, a flavoring, a surface active agent and a lubricant as a preparation prescription.
US20130058992 Gene expression signatures associated with response to imatinib mesylate in gastrointestinal stromal tumors and use thereof for predicting patient response to therapy and identification of agents which have efficacy for the treatment of cancer Compositions and methods are disclosed for identifying agents useful for the treatment of malignancy, particularly GISTs which are resistant to imatinib mesylate (IM). In a preferred embodiment, agents which sensitize cancer cells to IM are provided.
CN102895287A Preparation method of xylitol particles or tablets The invention discloses a preparation method of xylitol particles or tablets. A combination of nutrient factors consists of xylitol powder, a honeysuckle flower extract, calcium gluconate, vitamin A, vitamin D, vitamin C, stevioside and beta-cyclodextrin. The components are prepared into xylitol particles or tablets with the effect of preventing dental caries through a reasonable scientific formula and an advanced preparation process.
CN101352434A Use of triptolide in preparing medicament for treating c-KIT tyrosine kinase related tumor The invention relates to a purpose of a medicine which is prepared by triptolide and is used for curing tumor that is relevant to c-KIT tyrosine kinase. The invention verifies that a micromolecule natural product triptolide (TPL) can down-regulate the protein expression of D816V point mutation c-KIT for the first time, inhibit the phosphorylation thereof and induce the cell apoptosis of STI571 resistance c-KIT point mutation (D816). The invention discloses a novel micromolecule stayer of tyrosine kinase, more particularly overcomes the problem that the resistance property of the medicine STI 571 can be inhibited by the first-line tyrosine kinase that is used on the clinic at present. The TPL can be used for developing a novel specific medicine for curing tumors being relevant to c-KIT mutation, such as gastrointestinal stromal tumor, systemic mastocytosis and small cell lung cancer, etc.
US7097831 α-Amylase-resistant starch for producing foodstuff and medicaments The invention relates to foodstuff and animal feed which contain resistant starch on the basis of water-insoluble linear α-1,4-D-glucans. The invention also related to the utilization of resistant starch on the basis of water-insoluble linear α-1,4-D-glucans as medicaments.
WO2011093815A3 Pharmaceutical compositions comprising formoterol and mometasone The present invention relates to pharmaceutical compositions in dry powder form comprising formoterol and mometasone froate and/or their pharmaceutically acceptable derivatives as active agents, and capsule and blister forms containing these pharmaceutical compositions so as to be used in treatment of respiratory tract diseases.
CN1785198A Medicinal composite prepn. contg ranitidine hydrochloride and sucralfate A compound medicine for treating pyrosis, gastritis, indigestion, gastrointestinal diseases, etc is proportionally prepared from ranitidine hydrochloride and sucralfate.
CN103735620A Nano-emulsion in-situ gel for treating haemorrhoids The invention relates to nano-emulsion in-situ gel for treating haemorrhoids. The gel comprises the following components by weight: 30-100g of sophora flavescens, 30-120g of salviae miltiorrhizae, 30-100g of wild chrysanthemum, 1-8g of borneol, 1-8g of menthol, 30-160g of polyoxyethylated castor oil, 10-80g of absolute ethyl alcohol, 5-60g of isopropyl myristate, 60-160g of poloxamer 407, and 5-80g of poloxamer 188. The nano-emulsion in-situ gel can infiltrate into a mucous membrane to play the effects of clearing heat, removing toxicity, drying dampness, relieving itching, activating blood circulation to remove stasis, diminishing edema and relieving pain, and can be used for promoting local blood circulation, and improving nutrition of peripheral tissues to achieve the aims of diminishing edema and inflammation, and relieving pain.
US6943191 dihydroxy or diketoaromatic compounds; protein kinase inhibitors; antiproliferative activity Disubstituted lavendustin A analogs that are PTK inhibitors having antiproliferative activity are described. Preferred compounds of the disclosure, without limitation, satisfy either Formula 1 or Formula 2. The present disclosure also provides pharmaceutical compositions comprising effective amounts of disubstituted lavendustin A analogs and potentially comprising other active ingredients, other materials conventionally used in the formulation of pharmaceutical compositions, and mixtures thereof. The compounds and compositions of the disclosure can be used for treating subjects to, for example, inhibit the proliferation of living cells in the treatment of proliferative diseases.
US20100166898 Anti-bacterial use of extract from morus australis poir. and compound kuwanon h An extract prepared from the root barks of Morus australis Poir. and its use as an anti-bacteria agent, and use of a compound Kuwanon H having the following formula (I) separated from the extract as an anti-bacteria agent:
WO2014101038A1 Method for preparing drug-loaded microspheres A method for preparing drug-loaded microspheres comprises: providing an emulsifier; adding an organic mixed solution in the emulsifier to form a mixed solution; performing a first stirring step, so that emulsion droplets are formed and dispersed in an aqueous phase of the mixed solution; performing a second stirring step, so that a part of an organic solvent in the mixed solution volatilizes and the emulsion droplets in the aqueous phase of the mixed solution are solidified into solids; performing a separation step to separate the solids from the aqueous phase of the mixed solution; performing at least one rinsing step to rinse the solids using deionized water; and drying microspheres to obtain white solid powder.
CA2326654C Use of steroidal alkaloid derivatives as inhibitors of hedgehog signaling pathways The present invention makes available assays and reagents inhibiting paracrine and/or autocrine signals produced by a hedgehog protein or aberrant activation of a hedgehog signal transduction pathway, e.g., which involve the use of a steroidal alkaloid or other small molecule.
US20090312299 Isolated Isomers of Norelgestromin and Methods of Making and Using the Same The invention is directed to a process of preparing substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3E- and -3Z-oxime isomers, as well as a process for the synthesis of the mixture of isomers and the pure isomers. The invention also relates to substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime and substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer. Further aspects of the invention include a composition comprising substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime or substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer, and methods of treatment using said compositions.
CN101348461B N-(3-pyridine formyloxy)-3,5-dimethyl-1-amantadine for curing senile dementia or pharmaceutical salt thereof The invention relates to a N-(3-pyridine methoxy)-3,5-dimethyl-1-amine diadamantane for treatment of Alzheimer's Disease or a salt thereof for medicinal purpose, and also relates to the method for synthesizing the compound or the salt thereof for medicinal purpose, as well as the application in the preparation of drugs for treatment of Alzheimer's Disease, particularly, the compound is a synergetic prodrug produced through chemical coupling of amido link between nicotinic acid and amine diadamantane hydrochloric, on one hand, the prodrug not only avoids the side effects caused by nicotinic acid which is orally taken, but also implements cooperative dual effects on prevention and treatment of Alzheimer's disease by nicotinic acid and amine diadamantane, thereby improving the treatment effect of amine diamantine hydrochloric on Alzheimer's Disease; on the other hand, the enhanced molecular solubility of amine diadamantane in lipid facilitates the passage of the prodrug through a blood-brain barrier, increases the distribution concentration of the prodrug in the cerebrospinal fluid, thereby accomplishing the aim of reducing the peripheral side effects of the drug.
WO2007110649A3 Process for the preparation of 2,6,9-trisubstituted purines The present invention relates to a process for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R2 is (a) where R3, R4, R7 and R8 are each independently selected from H, alkyl, aryl and aralkyl, said alkyl, aryl and aralkyl groups each being optionally substituted with one or more R12 groups, and wherein at least one of R3, R4, R7 and R8 is other than H; R5 is OH, O-alkyl, NH2, H, alkyl, aryl or aralkyl, said alkyl, aryl and aralkyl groups each being optionally substituted with one or more R12 groups; R6 is NR10R11, wherein R10 and R11 are each independently H or hydrocarbyl; R9 is hydrocarbyl; and each R12 is independently selected from OR13, halo, alkyl, COOR14, CONR15R16, SO2NR17R18, NO2, CN, NR19R20SR21 and CF3, where R13-21 are each independently H, alkyl or aryl; said process comprising the steps of (II) (III) (IV) (i) converting a compound of formula (II) to a compound of formula (III), wherein X is halo and R is aryl, alkyl, cycloalkyl, aralkyl, heteroaryl or alkyl-heteroaryl; (ii) converting said compound of formula (III) to a compound of formula (IV); and (iii) converting said compound of formula (IV) to a compound of formula (I).
WO2014088281A1 Novel method for preparing cabazitaxel from 10-deacetylbaccatin iii in high yield, and novel intermediate therefor The present invention relates to a novel method for preparing cabazitaxel from 10-deacetylbaccatin III, and a novel intermediate therefor, and more specifically, to: a method which allows cabazitaxel to be more easily prepared in a high yield and in a high purity within a short time compared with a conventional method by preparing cabazitaxel via a novel intermediate using 10-deacetylbaccatin III as a starting material, and thus is suitable for industrial mass production; and a novel intermediate therefor.
US6841579 To screen for inhibitors of cell growth and to develop small molecule therapeutics for treating cancers The present invention relates to AUR1 and/or AUR2 polypeptides, nucleic acids encoding such polypeptides, cells, tissues and animals containing such nucleic acids, antibodies to such polypeptides, assays utilizing such polypeptides, and methods relating to all of the foregoing. Methods for treatment, diagnosis, and screening are provided for AUR1 and/or AUR2 related diseases or conditions characterized by an abnormal interaction between a AUR1 and/or AUR2 polypeptide and a AUR1 and/or AUR2 binding partner.
CN102078309A Dispersible tablet containing antipsychotic medicines and application thereof The invention relates to a novel dispersible tablet which is prepared from a certain amount of antipsychotic medicines or pharmaceutically acceptable salt or ester thereof or mixture thereof, a certain amount of selective serotonin reuptake inhibitors (SSRIs) and at least one of pharmaceutically acceptable carriers, wherein the antipsychotic medicines are aripiprazole, fluvoxamine, escitalopram, olanzapine, mirtazapine, clozapine, ziprasidone, mianserin, agomelatine, lurasidone, iloperidone, blonanserin, moclobemide, timiperone, palipeddone, trimipramine, carpipramine, lofepramine or mosapramine. The novel dispersible tablet is used for preventing, delaying or treating depression or schizophrenia of patients. Compared with common tablets or capsules, the novel dispersible tablet has the characteristics of quick and uniform dispersion, short disintegration time, quick medicine absorption, high bioavailability and good stability, and is convenient to take.
CN1582939A Dioxyimipramine hydrochloride drops and their preparation A dripping pill of dioxopromethazine hydrochloride is prepared by superfine pulverizing and conventional process for preparing dripping pills.
CN103172548A Preparation method and application of methanesulfonamide compound The invention relates to a preparation method and an application of a methanesulfonamide compound, and in particularly provides a methanesulfonamide compound. The methanesulfonamide compound has a structure as shown in the general formula (I), and can well inhibit the survival and growth of SUM-159, HCC-1954 and MCF-7 cells, wherein R is hydrogen, a C2-C6 linear chain or branched alkane, an allyl group, trifluoro-alkyl, cyclopropyl, or other components as shown in the specification.
CN101411716A Use of polygonin for preparing product for resisting dementia The invention relates to application of polydatin which is an extract of polygonum cuspidatum. In-vitro researching experiments show that the polydatin has strong protecting effect for pathological injuries caused by rats multiple infarctional cerebral ischemic injuries, can significantly improve learning memory function of dementia model rats, so the polydatin can be used for preparing a product for resisting vascular dementia and a product, particularly a medicine for resisting senile dementia. The modes for using the polydatin include independent use, or combined use with other chemical substances. Dementia is a key disease impacting health of the elderly, particularly, frequency of disease development of the vascular dementia and the senile dementia is significantly increased to seriously threaten health and life of human beings. The invention provides a novel drug source for clinically treating the vascular dementia and the senile dementia, and has important value for developing and utilizing medicinal plant resource in China.
US8367655 Pyridoindolobenzox—and thiazepine derivatives and uses thereof The present invention discloses pyridoindolobenzox- and thiazepine compositions of Formula 1, wherein A is —CH(R9)—X—, —XCH(R9)—; —CO—X— or —X—CO—; X is —O—, —S—, —SO—, or —SO2—. Y is a single bond or a double bond. D and E are independently —(CH2)n—; and ‘n’ varies from 0 to 2. R1 to R9 are various electron donating, electron withdrawing, hydrophilic, or lipophilic groups selected to optimize the physicochemical and biological properties of compounds of Formula I.
US7168597 Aerosol metering valve A metering valve that includes a valve body defining a metering chamber having an inlet valve adapted to be reversibly actuable from an open position to a closed position located at the inlet, and an outlet valve adapted to be reversibly actuable from a dispensing to a non-dispensing position located at the outlet, where the outlet valve includes an outlet valve seat adapted to be in biasable contact with an outlet valve poppet is described. Aerosol containers and inhalation devices that include such metering valves are also described, as are methods of using such inhalation devices.
CN101966173A Medicinal use of dinitrobenzoylsilybin for preparing glycosidase inhibitor The invention relates to medicinal use of dinitrobenzoylsilybin for preparing a glycosidase inhibitor, in particular discloses use of 3,5-dinitrobenzoyl substituted silybin ester type flavonolignan and pharmaceutically acceptable salts thereof for the preparation of medicaments for inhibiting alpha-glucuroide and controlling type 2 diabetes. The flavonolignan has extremely obvious activity for inhibiting alpha-glucuroide and has the activity strength for inhibiting the alpha-glucuroide of 71.19 percent at the concentration of 40mg/ml, and by measuring median inhibitory concentration, the strength of the flavonolignan for inhibiting the alpha-glucuroide is 9.5 times that of a positive control medicament acarbose. Pharmacodynamic results prove that the flavonolignan or the pharmaceutically acceptable salts thereof can be expectedly used as a glycosidase inhibitor medicament, particularly a medicament for controlling the type 2 diabetes.
CA1341478C Therapeutic methods using catalytic antibodies Antigens capable of eliciting antibodies which can catalyze chemical reactions, in particular, the cleavage or formation of a peptide linkage, comprising a hapten or a hapten and a suitable carrier molecule are disclosed. Haptens include, among others, silicon and boron containing compounds. antibodies which are catalytically active for chemical reactions, in particular, the cleavage or formation of an amide, peptide, ester, or glycosidic bond, and which are elicited by such antigens are disclosed as well as methods for producing the antibodies, methods for catalyzing the cleavage or formation of an amide, peptide, ester, or glycosidic bond in a biomolecule, and methods for treating a variety of diseases using antibodies.
CN101264095A Application of polydatin in preventing and controlling obesity and relieving insulin resistance The invention provides uses of polydatin active substance in preparing medicinal composition, food composition, health-care composition and/or dietary addition agent, wherein, the compositions are used for preventing, controlling or curing the diseases relatively to insulin resistance and/or symptoms or disease relatively to obesity. The invention also provides a method for losing weight by using polydatin active substance or the composition, as well as a composition which comprises polydatin active substance and other substances for preventing, controlling or curing the diseases relatively to insulin resistance and/or symptoms or disease relatively to obesity. The compositions of the invention have the advantages of high safety, good acceptability for market, high solubility, easy absorption and good stability.
CN101575330A Novel voriconazole broad-spectrum antifungal medicine compound, broad-spectrum antifungal medicine composition and application thereof The invention relates to a novel broad-spectrum antifungal medicine compound, a broad-spectrum antifungal medicine composition, an application of the compound or the composition in the preparation of a broad-spectrum antifungal medicine, and an application of the compound or the composition in the preparation of a medicine used for treating severe invasive infection (comprising Candida krusei) caused by invasive aspergillosis and/or Fluconazole-resistant Monilia and/or severe infection caused by Scedosporium and fusarium. The novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition have extensive and strong antifungal activity and better dynamic property and safety. For deep mycotic infection, the novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition are better than the original voriconazole in the aspects of the antibiotic activity and the medicine resistance and is better than amphotericin B in the aspects of safety and effectiveness; and compared with the formerly applied voriconazole, Fluconazole, itraconazole and amphotericin B, the novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition have reinforced medicine effect, less adverse reaction and good safety.
CN102861093A Application of Houttuynoid B in medicine for treating colorectal cancer The invention discloses application of Houttuynoid B in preparation of a medicine for treating colorectal cancer, belonging to the technical field of new application of medicine. The invention discovers that Houttuynoid B has the remarkable inhibitory effects on the growth of human colorectal cancer cell strains including LOVE1, LoVo, SW620 and SW480 through the evaluation of in vitro MTT antineoplastic activity. Therefore, Houttuynoid B can be used for preparing the anti-colorectal cancer medicine and has good development and application prospects. The application of Houttuynoid B in preparation of the medicine for treating colorectal cancer provided by the invention is disclosed firstly. The skeleton type belongs to new skeleton type, and the inhibitory activity of Houttuynoid B on colorectal cancer cells is unexpectedly strong.
EP1294370B1 Triterpenoid derivatives The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in therapy. Preferably, the compound may be used for treating a patient suffering from leukaemia, cancer or other proliferative disorder. A further embodiment relates to the use of a compound of formula (I) in an assay for detecting the phosphorylation and acetylation state of cellular substrates. The present invention also relates to novel compounds of formula (Ia).
US20120052058 Methods of managing the blood coagulation and pharmaceutical compositions related thereto The disclosure relates to methods of managing blood coagulation and pharmaceutical compositions related thereto. In certain embodiments, the disclosure relates to methods of managing the coagulation of blood in a patient undergoing surgery comprising administering combinations of a direct thrombin inhibitor and a coagulation factor inhibitor. In some embodiments, the disclosure relates to treating or preventing clotting by administering compositions disclosed herein to a subject at risk for, exhibiting symptoms of, or diagnosed with a blood clot.
US20120142759 Soluble thf receptors and their use in treatment of disease The present invention relates to splice switching oligonucleotides or splice switching oligomers (SSOs). The preferred SSOs according to the invention target exon 7 of TNFR1 (TNFRSF1A) or TNFR2 (TNFRSF1A) pre-mRNA, typically resulting in the production of TNFR variants which comprise a deletion in part or the entire exon 7 respectfully. SSOs targeting exon 7 are found to result in a soluble form of the TNFR, which has thereputic benefit for treatment of inflammatory diseases. The SSO's are characterized in that they are substantially incapable or incapable of recruiting RNaseH.
WO2012147619A1 Blood glucose level increase inhibitor The purpose of the present invention is to provide a blood glucose level increase inhibitor. The purpose of the present invention is also to provide a composition for preventing or treating lifestyle diseases and disorders related thereto. The present invention relates to a blood glucose level increase inhibitor comprising a compound represented by formula (I), as well as a proanthocyanidin. The present invention also relates to a composition for preventing or treating lifestyle diseases and disorders related thereto, the composition containing a compound represented by formula (I), as well as a proanthocyanidin.
WO2007087667A2 Combination preparation for improving sperm quality The invention relates to a combination preparation for improving the sperm quality and capacitation of a male individual. Said combination preparation comprises effective amounts of L-carnitine, coenzyme Q10, at least one vitamin E, particularly α-tocopherol, at least one source of zinc, especially zinc sulfate or zinc chloride, at least one source of vitamin B, particularly folic acid, at least one source of selenium, glutathione, and arginine or salts or derivatives thereof as active substances.
EP1140196B1 pharmaceutical solutions comprising triphenylethylene antiestrogens The invention relates to aqueous compositions of nonsteroidal triphenylethylene antiestrogens for pharmaceutical use comprising as a solubility enhancing agent a pharmaceutically acceptable mono- or dicarboxylic acid having 1-5 carbon atoms, wherein the carbon chain may further contain 1-4 hydroxyl, 1-3 oxo, or one or several halogen substituents, or a corresponding anion thereof, or methanesulfonic acid or its corresponding anion, in molar excess with respect to the triphenylethylene antiestrogen, optionally together with an organic water miscible co-solvent such as polyethylene glycol (PEG), propylene glycol, ethanol or isopropanol.
WO2007082866A3 Use of chavicol for the treatment of superfinfected oily skin and scalp Chavicol has been found to possess a dual-action in the treatment of superinfected oily skin and scalp by sebum reduction coupled with biocidal activity on lipophilic anaerobic micro-organisms, whilst possessing no significant estrogenic nor sensitizing potentials. It is thus indicated for the manufacture of orally or topically administrable compositions for the treatment of superinfected oily skin and/or scalp and, in particular, for the treatment of androgenic disorders of skin and/or scalp such androgenic disorders incude alopecia, acne, seborrhea and/or dandruff.
US8093229 Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors Alkynyl pyrrolo [2,3-d] pyrimidines of Formula I are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such compounds are also described and claimed.
WO2008141438A1 Gabaergic modulators for treating airway conditions The present disclosure provides uses, methods and compositions comprising GABAergic modulators such as antisense nucleic acids, antibodies or drugs for treating airway conditions in an animal. Airway conditions include conditions such as asthma, or conditions comprising altered mucus production.
CN101481688B SiRNA for inhibiting human KCTD1 gene expression and use thereof in pharmacy The invention discloses a siRNA for inhibiting human KCTD1 gene expression and an application thereof in the pharmacy industry. In the invention, based on RNA interference technology, a cDNA sequence of a human KCTD1 gene is obtained from GenBank, according to the basic principle of siRNA target sequence selection, 21 ribonucleotide is designed and synthesized by a chemical method in connection with KCTD1 gene. The invention can efficiently and specifically inhibit mRNA and protein level expressions of the KCTD1 gene and specifically ease the inhabitation of the transcription activity of a transcription factor AP-2 by the KCTD1, thus the invention is applicable for preparing the drugs of resisting breast cancer.
US20130108672 Pharmaceutical compositions for substituted quinazolinones The present disclosure relates to novel solid pharmaceutical formulations and process for their preparation. The present disclosure also provides, in part, methods of using the pharmaceutical formulations for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
US20090286867 Compositions and methods of administering doxepin to mucosal tissue Compositions and methods for pain relief involve delivery of doxepin to mucosal tissue. Vehicles for administering doxepin may be formulated for sustained release and/or site-specific application to maximize beneficial pain relief locally while minimizing significant adverse side effects.
WO2007052794A1 o-SUBSTITUTED ANILINE DERIVATIVE AND ANTIOXIDANT DRUG A compound or salt thereof which has antioxidant activity and is effective in the treatment of ischemic organ diseases including arteriosclerosis, heart infarction, and brain infarction, in the treatment of diseases caused by oxidative cellular disorders, such as kidney diseases, and in the inhibition of retinal disorders caused by oxidation due to light, etc. Also provided is an antioxidant drug containing at least one of the compound and salt as an active ingredient. The compound is represented by the formula (1). The antioxidant drug is characterized by containing at least one of the compound and salt as an active ingredient. {In the formula (1), a is 1 or 2, R0 represents (un)substituted amino, R1 to R4 each independently represents hydrogen or alkyl, E represents an (un)substituted alkylene chain, D represents a single bond, oxygen, (un)substituted nitrogen, sulfur, sulfinyl, sulfonyl, carbonyl, carbonylamino, or aminocarbonyl, and A represents an (un)substituted aromatic hydrocarbon group, (un)substituted heterocyclic group, (un)substituted aralkyl, or (un)substituted heteroaralkyl.}
US20110200667 Veterinary pharmaceutical formulacion that comprises an rna recombinant particle that encodes for a cu/zn superoxide dismutase protein of ruminant pathogenic bacteria and at least one rna alphavirus belonging to the semliki forest virus family The technology is a veterinary pharmaceutical formulation of two vaccines, one from an RNA viral vector system constituted by an RNA recombinant particle that codifies for a Cu/Zn superoxide dismutase protein of Brucella abortus, and the other based on naked RNA constituted by a recombinant molecule of naked RNA that carries a sequence for the synthesis of at least one recombinant Cu/Zn superoxide dismutase protein of Brucella abortus and some Semliki Forest virus genes. An expression system based on the Semliki Forest virus and a use of this system, in addition to a method for the preparation of the pharmaceutical formulations.
CN101717407A Highly substituted alpha-amino phosphonate derivative as well as preparation method and medical application thereof The invention relates to a highly substituted alpha-amino phosphonate derivative as well as a preparation method and a medical application thereof. Particularly, the invention provides a compound expressed by the general formula I, a derivative, a tautomera, a despinner or an optical isomer, a medical salt or a solvent compound, a medicament combination, a preparation method and an application of the compound to preparing a medicament for preventing or treating autoimmune diseases which are relevant to immune system dysfunction, such as chronic nephritis, multiple sclerosis, psoriasis, systemic lupus erythematosus, chronic infectious arthritis, insulin-dependent diabetes, chronic toxic thyroiditis, myasthenia gravis, ankylosing spondylitis, pemphigus, and the like and organ transplantation and anaphylaxis diseases or an application of the compound used as a tool medicament for researching diseases which are relevant to the immune system function or dysfunction.
CN103638006A Application of Oleaceran in medicine for lowering blood glucose The invention discloses application of Oleaceran in medicine for lowering blood glucose. The application of Oleaceran disclosed in the invention is proved to have evident anti-diabetic effect; the Oleaceran is a compound having definite chemical structure, belongs to a brand new skeleton type, and has strong glycuresis prevention and treatment activity; the Oleaceran has outstanding substantive features and has an obvious progress in the treatment or resisting of glycuresis.
CA2140441C Inhibitors of c-amp phosphodiesterase and tnf This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase. Compounds according to the invention are of formula Iwhich has the following general chemical structure:
CN101204541A Preparation strengthening breeding function of male raccoon dog and fox The invention relates to a strengthening agent for reproductive capacity of foxes and raccoon dogs, which belongs to the field of animal nutrition and reproductive technology.Every 100g product consists of 20-30g of soybean flour, 15-20g of fish powder, 8-12g of algae powder, 10-15g of yolk powder, 3-8g of Chinese onion seed powder, 2-6g of Chinese chive seed powder, 0.8-1.5g of linoleic acid, 100-500mg of vitamin E, 100-200mg of methionine manganese, 300-800mg of methionine zinc, 50-100mg of lysine selenium and 1.5-4.0g of vitamin complex , the rest is corn-meal. The invention can supply the foxes and raccoon dogs with sufficient nutrition, improve development of reproductive organs of the foxes and raccoon dogs, promote secretion of androgen, increase sperm motility, survival rate and fertilization rate, reduce sperm abnormality rate and enhance reproductive capacity of male foxes and raccoon dogs.
CN101643490B Epothilonoside compound, preparation method and application as cytostatics thereof The invention relates to epothilonoside, in particular to epothilonoside A, epothilonoside B, epothilonoside C, epothilonoside D and epothilonoside E. The invention also relates to preparation methods and application as cytostatics thereof.
US7297353 For oral administration, injection and topical application; can eliminate the aseptic inflammations, edema, adhesion caused by aseptic inflammations, and stubborn pain, complex body disorders caused by aseptic inflammation, edema and adhesion The present invention discloses a medicament useful for treating aseptic inflammations, containing anemonin as an effective ingredient, and use of the anemonin compound in treating aseptic inflammations. The effective ingredient in the present medicament, anemonin, can be extracted and separated from natural plants containing anemonin or its precursor. The present invention also discloses a method for preparing anemonin extract. The present medicament can be formulated into preparations for oral administration, injection and topical application, especially liquid extract, plaster, suppository, liniment, and paint etc., which can be transdermally absorbed.
US7235536 Administering sulfated polysaccharide such as cellulose sulfate, dextran sulfate, dermatan sulfate, chondroitin sulfate, pentosan sulfate, fucoidin, mannan sulfate, dextrin sulfate, curdlan sulfate, chitin sulfate, heparin or heparin sulfate for therapy and prophylaxis of fungal infection The invention relates to the treating, inhibiting or preventing of certain infectious agents including papilloma virus and various vaginitis-causing microbes by employing cellulose sulfate and other sulfated polysaccharides. In one embodiment, the method involves preventing, inhibiting or treating fungal infections. Corresponding methods of use in manufacturing a medicament as well as use in preventing and inhibiting various infectious agents as well as malignant lesions are disclosed. In another embodiment, use of a sulfated polysaccharide in preventing, inhibiting or treating a parasitic infection is disclosed.
EP1747231A1 Aminosulphonyl- or aminosulphonylamino-substituted phenyl esters as estriol and estetrol prodrugs The invention relates to estriol and estetrol prodrugs of general formula (I), in which group Y is bonded to the steroid, the method for production thereof, pharmaceutical compositions comprising said compounds and the use thereof for production of medicaments with estrogenic effect.
EP2357166A1 Auto magnetic metal salen complex compound The present invention provides a drug using the magnetic properties of a metal salen complex as represented by the following general formula in order to magnetize the intended drug by chemically binding the drug to a metal salen complex so that the drug can be delivered to the target diseased site. The drug can be delivered to the diseased site using the magnetic properties of the drug per se without using a carrier made of a magnetic substance as in the conventional methods.
CN103704709A Dispersible tablet of codonopsis pilosula and bergamot and preparation method of dispersible tablet The invention discloses a dispersible tablet of codonopsis pilosula and bergamot. The dispersible tablet comprises the following components in parts by weight: 200-300 parts of Chinese yam, 200-300 parts of Chinese angelica, 200-300 parts of the codonopsis pilosula, 100-200 pats of the bergamot, 40-60 parts of microcrystalline cellulose, 0.12-0.32 part of trametes versicolor extract, 0.12-0.32 chitosan, 1-2 parts of vitamin C, 0.1-0.2 part of calcium carbonate, 100-170 parts of mannitol, 10-15 parts of sucralose, 10-50 parts of superfine silica powder, 3-5 parts of carboxymethylcellulose, 55-80 parts of sodium carboxymethyl starch, and 4-6 parts of magnesium stearate. The dispersible tablet has the effects of enriching blood and replenishing qi, increasing the bone mineral density, enhancing the immunity and the like. The dispersible tablet is suitable for postpartum abdominal pain, and the symptoms include gripping pain of the lower abdomen, comfortable feeling when the lower abdomen is pressed, little and light lochia, dizziness, tinnitus, fence dregs, pink tongue, thin fur and the like; the dispersible tablet is used for auxiliary rehabilitation.
CN102115482A Annatto oligosaccharide, preparation method and usage thereof The invention relates to an annatto oligosaccharide which contains annatto tetrose with the mass of more than 40% of the total mass, wherein the annatto tetrose has the structural formula of alpha-D-Gal-(1-3)-alpha-D-Gal-(1-6)-alpha-D-Glc-(1-2)-beta-D-Fru. The preparation method of the annatto oligosaccharide and the annatto tetrose is simple in structure and high in product purity, has the activity of strengthening the immunity, adjusting intestinal flora and improving gastrointestinal tract functions, and is free from toxic side effect.
CN1943589A Injection for positioning and promoting fat growth and its preparing method Said invention, injection of orientation promoting fat growth comprises composite particles which is consisted of magnetic particles being covered with or absorbing special medication whereby promoting fat growth, in 100ml water solution, contents thereof is, Fe3O4 magnetic particles 0.5-2g,component of special medication acetyl-coA 0-1g, NADP 0-1g, citrate 0-8g. Preparation of said injection is, making magnetic particles centrifugal and washing by distilled water, adding certain volume of special medicinal water soluble described hereinabove, density of each component is seen hereinabove, making thereof mixed evenly, in ultrasonic handling for several min.; again heating to 40-100deg.C for 5-30 min. finally sterilization by high temp and pressure.
CN101904861A Application of Saccharomyces cerevisiae RNA in preparing medicine for promoting biologic metabolism and immunity The invention discloses an application Saccharomyces cerevisiae RNA in preparing a medicine for promoting biologic metabolism and immunity. Saccharomyces cerevisiae RNA 25s and 18s sequences and human RNA 28s and 18s sequences are highly homological, so the sequences have high homogeny, high compatibility and high safety and can be easily absorbed and utilized by human body. The Saccharomyces cerevisiae RNA can facilitate the synthesis of the ribosomal DND nucleate of human body so as to activate the biologic metabolism and promote immunity.
EP1196431B1 A substantially crystalline form of melagatran There is provided melagatran in a form which is substantially crystalline. It has been found that crystalline forms of melagatran have a high chemical and solid state stability when compared to amorphous forms of the compound.
US20090098189 Azaindoles as inhibitors of soluble adenylate cyclase The present invention relates to azaindoles of general formula I, a method for the production thereof, and to the use thereof for the production of pharmaceutical compositions.
CN1935802A Armiharisin succinic mono ester with cholagogic effect, and its salt and medicinal composition The invention relates to an Armillarisinum hemisuccinate and the preparing method and use thereof. And it can be made by acylation reaction of Armillarisinum and succinic anhydride; besides, the invention also relates to its pharmaceutically acceptable salts, such as K salts, Na salts, Ca salts and Mg salts, as well as the salts formed of it and basic amino acid, including lysine and arginine salts. And the pharmacological experiments indicate it has obvious cholagogue effect. And the combination of it or its pharmaceutically acceptable salts as active components and corresponding medicinal dressing can be made into oral and intravenous preparations for curing acute cholecystitis, acute attack of chronic cholecystitis, acute biliary passage infection (including calculus type and parasite type), and acute and chronic hepatitides.
CA2417190C New beta-amyloid inhibitors, processes for preparing them and their use as pharmaceutical compositions The present invention relates to compounds of general formula (I) (see formula I) wherein the groups A, Het, R1, R2 and R3 may have the meanings given in the description and in the claims, processes for preparing them and the use of compounds of general formula (I) as pharmaceutical compositions, particularly as pharmaceutical compositions with a beta-amyloid-inhibiting activity.
CN1843346A Pharmaceutical composition containing paclitaxel analog compound and its preparation method The invention relates to a medicinal composition containing Paclitaxel compounds, wherein the medicinal composition comprises 5-75% of phospholipids, 0.01-50% of interfacial active agent with HLB greater than 10, 0.01-50% of alcohol compounds, and 0.01-40% of Paclitaxel compounds or their derivatives. The invention also provides a process for preparing the medicinal composition containing Paclitaxel compounds.
WO2013059791A2 Methods and compositions for promoting axon regeneration and nerve function Provided are methods for promoting axon regeneration of a Central Nervous System (CNS) neuron and promoting nerve function following injury to a CNS neuron, for example, brain and/or spinal cord injury. Axon regeneration in a CNS neuron or nerve function following injury to a CNS neuron can be promoted by administering a necrosis inhibitor either alone or in combination with an apoptosis inhibitor to a subject suffering from a CNS disorder, wherein a symptom of the CNS disorder is axon degeneration.
CN103705941A Calcipotriol beta-cyclodextrin inclusion compound and preparation method thereof The invention relates to a calcipotriol beta-cyclodextrin inclusion compound and a preparation method thereof. The inclusion compound comprises 4.5%-21% of calcipotriol. The preparation method comprises step of adding one volume of 0.3mol/L calcipotriol ethanol solution into 15-20 volumes of 0.012-0.016mol/L beta-cyclodextrin aqueous solution for clathration. The preparation method finally prepares the calcipotriol inclusion compound meeting the requirement of medicines in grain size and uniformity. The inclusion compound can be further prepared into cream, ointment and suspension solution. Compared with non-covered calcipotriol, the calcipotriol beta-cyclodextrin inclusion compound and the preparations prepared from the inclusion compound are remarkably improved in stability, and the problem of uneven content caused by trace feeding capacity is solved.
WO2005100990A3 Diagnostics and therapeutics for diseases associated with purinoceptor 2 type y (p2y2) The invention provides a human P2Y2 which is associated with the cardiovascular diseases, dermatological diseases, endocrinological diseases, metabolic diseases, cancer, gastroenterological diseases, inflammation, hematological diseases, respiratory diseases, muscle skeleton disorders, neurological diseases and urological diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular diseases, dermatological diseases, endocrinological diseases, metabolic diseases, cancer, gastroenterological diseases, inflammation, hematological diseases, respiratory diseases, muscle skeleton disorders, neurological diseases and urological diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of P2Y2 as well as pharmaceutical compositions comprising such compounds.
CA2685473A1 Treatment of virally induced lesions The present invention relates generally to the treatment of cutaneous lesions containing cells infected by a virus, as well as compositions for the treatment of such lesions. More specifically, the invention relates to the use of ingenol compounds, particularly ingenol angelates, in treating lesions caused by infection with a papilloma virus, such as a mammalian papilloma virus, in particular a Human Papilloma Virus.
WO2007084332A3 Memantine for the normalization of visual acuity deficits A method for the treatment of disturbance of visual function which comprises administering a pharmaceutically effective amount of memantine to a patient in need of treatment of said disturbance.
WO2011078370A1 Novel parabanic acid derivative and drug having the same as active ingredient Provided is a novel compound which has a strong AMPK activating action and a favorable effect derived from the AMPK activating action in vivo, and further provided is a drug which is structurally novel and highly effective, long-acting, and safe as a type II diabetes drug. As a result of focusing on the specific role of human AMPK in energy metabolism in order to create a drug that is structurally novel and highly effective, long-acting, and safe as a type II diabetes drug, it was discovered that the novel benzylparabanic acid derivative represented by general formula (1) and addition salts thereof have an excellent human AMPK activating action and an excellent blood glucose-lowering action and lipid-lowering action in vivo.
WO2013093940A1 Nitrofurfuryl substituted phenyl linked piperidino-oxadiazoline conjugates as anti-tubercular agents and process for the preparation thereof The present invention provides nitrofurfuryl substituted phenyl linked piperidino-oxadiazolone compounds of general formula (A) as anti-tubercular agents; wherein G= formula (B); X=H, F; R=H, CH3, C2H5, Benzyl.
US8344025 Oxalic acid derivatives and use thereof as physiological cooling active ingredients The present invention relates to specific oxalic acid derivatives and to corresponding mixtures and to uses thereof as physiological cooling active ingredients.
WO2008058383A1 Acat inhibitors and their use in the prevention or treatment of fibrosis The present invention relates to the use of ACAT inhibitors, {e.g. F-1394, Avasimibe (CI-1011), Pactimibe (CS505), Efluimibe (F12511), Eldacimibe, NTE 122, AS-183, KW-3033, E5324, FY087, FCE27677, CI-976, K-604, TEI6522, Octimibate, FR179254, and S 58-035, or mixtures thereof), compositions comprising the same, and methods for preventing or treating fibrosis, for preventing or reducing collagen deposition in a tissue, and in the prevention and reduction of excessive fibrous connective tissue
CN101899004A Sinomenine derivatives and preparation method and medical application thereof The invention provides sinomenine derivatives and preparation methods and medical applications thereof and relates to the pharmaceutical chemistry field. The invention particularly relates to a sinomenine derivative with the structural general formula I. The invention also discloses the preparation method of the sinomenine derivative. The invention selects the 293 cell transfected by Phf-Kb-luc to test the inhibitory action of the compounds to NF-kB signal channel and the results show that most of the compounds have good inhibitory action. Therefore, the sinomenine derivatives can be used to prepare anti-inflammatory immune medicines.
CN102068450B Application of aucubin to preparation of anti-thrombosis medicament The invention relates to the application of aucubin to the preparation of an anti-thrombosis medicament, and discloses the application of the aucubin to the preparation of the anti-thrombosis medicament and the anti-thrombosis medicament taking the aucubin as an active ingredient, which belong to the technical field of medicament preparation. The medicament comprises the following components in part by weight: 10 to 99 parts of aucubin and 1 to 90 parts of pharmaceutically acceptable carrier. In the invention, researches show that the aucubin has an effect on the suppression of platelet aggregation caused by adenosine diphosphate (ADP), and the application is different from the conventional reported use of the aucubin. A new way for preventing and treating thrombosis caused by the platelet aggregation is provided.
US20110053946 Aryl-Quinolyl Compounds and Their Use The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain aryl-quinolyl compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.
CN101065485A LNA oligonucleotides and the treatment of cancer The present disclosure concerns LNA oligonucleotides having a (sub)sequence of the general formula 5'- ( Me Cx )(Tx,) Me CXAs Astscscsastsgsgs MeCXAX (G x) (c)-3',and preferably of the general formula 5'- Me C XTX), MeCXAsastscscsastsgsgs Me CxAx G x c-3', wherein capital letters designate a n LNA nucleotide analogue selected from .beta. -D-oxy-LNA, .beta. -D-thio-LNA, .beta.-D-amino-LNA and a-L-oxy-LNA, small letters designate a deoxynucleotid e, and underline designates either an LNA nucleotide analogue as defined above or a deoxynucleotide. Such LNA oligonucleotides exhibit surprisingly good properties with respect to inhibition of the expression of Survivin by means of an anti-sense mechanism, and thereby lead to reduction or inhibition of tumour development in vivo. The LNA oligonucleotides are superior to other L NA oligonucletides targeting Surviving mRNA measured by functional read outs su ch as apoptosis induction and proliferation inhibition, and is potent in down- regulating Survivin mRNA and protein in transfected cancer cell lines, and induce apoptosis in combination with Taxol superior compared to other LNA oligonucleotides.
CN103319449A 1,2,3,6,7-pentahydroxydiphenylpyrrone derivative and its preparation method and application thereof The invention relates to the technical field of medicinal chemistry, especially to a 1,2,3,6,7-pentahydroxydiphenylpyrrone derivative and its preparation method and an application thereof. The compound with a structure as shown in the formula I inhibits xanthine oxidase activity and promotes uric acid excretion so as to reduce uric acid level in blood. Thus, therapeutical effect of treating hyperuricemia is achieved, and a new option for clinic treatment of hyperuricemia is provided. In addition, the preparation method of the compound with the structure as shown in the formula I is simple and easy to operate, and has advantages of good reappearance and little environmental pollution.
CA2712747A1 Combinatory cancer treatment The present invention relates to a pharmaceutical composition for treating a neoplasm, a preneoplasm, a proliferative disorder and/or a precancerous lesion, the use of such compositions for the treatment of the listed conditions, and methods of treating the listed conditions. The composition of the present invention comprises an inhibitor of elF4E, a methyltransferase inhibitor, and a pharmaceutically acceptable carrier.
CN103012356A Compound with alpha-glycosidase inhibitory activity, as well as preparation method and application of compound The invention discloses a compound with alpha-glycosidase inhibitory activity, as well as a preparation method and application of the compound. The structure of the compound is shown as formula I. The preparation method of the compound comprises the following steps: swertia mussotii is percolated and extracted by ethyl alcohol with concentration of 50-95 percent, extract is compounded, the ethyl alcohol is removed via rotary evaporation, and concrete is obtained after drying; the concrete is dissolved in water and extracted by dichloromethane; extract of the dichloromethane is separated by adopting a silica gel column color spectrum and eluted by petroleum ether-acetic ether in a gradient mode, and 8 coarse fractions are obtained by combining eluant according to the size of the polarity of the compound displayed by thin-layer chromatography in an ascending order and are respectively marked from F1-F8; compounds ZYC-01 and ZYC-02 are prepared by the coarse fraction F3 via combing the silica gel column chromatography and preparative efficient liquid-phase chromatographic fractionation; ZYC-04 is obtained via the coarse fraction F4; and ZYC-03 and ZYC-05 are prepared and obtained by the coarse fraction F5 via gel column chromatography. Traditionally, the swertia mussotii is mainly used for researching and developing anti-hepatitis drugs. The compound with the alpha-glycosidase inhibitory and the application of the compound to drugs for curing diabetes are reported for the first time.
EP1647549A1 Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.
EP1280781B1 5-ht 7 receptor antagonists Amino-pyrimidine and amino-triazine derivatives having 5-HT7 antagonist activity for the treatment of sleeping disorders, depression, schizophrenia, anxiety, obsessive compulsive disorders, circadian rhythm disorders, ocular disorders and/or centrally and peripherally mediated hypertension are provided.
US8273728 Preformulation for tabletting natural mixtures of conjugated estrogens A pharmaceutical preformulation in the form of a solid, free-flowing dry extract of a natural mixture of conjugated equine estrogens, which is particularly suitable use in for solid galenic forms, e.g. tabletting. The conjugated estrogens are available for further galenic processing in a form which assures the chemical stability of the hormones and permits advantageous processing into solid galenic forms, for example a tablet. The invention furthermore relates to a method for producing these preformulations in the form of a dry extract.
US20080249171 Administering diacylglycerols to accumulate fatty acids in the small intestine to suppress biosynthesis of triacylglycerols; antidiabetic agents; insulin resistance; lower blood remnant/leptin level, enhancement of beta -oxidation and uncoupling protein (UCP) expression to promote energy consumption Disclosed are a method for activating lipid metabolism in the small intestine epithelium and also a method for promoting accumulation of fatty acids into the small intestine epithelium, each of which features administering an effective amount of a diacylglycerol. Also disclosed are methods for improving various symptoms in diabetes, which have ingesting a diacylglycerol. Ingestion of the diacylglycerol leads to accumulation of the fatty acids in the small intestine. The fatty acids so accumulated promote induction of β-oxidation, thereby not only activating lipid catabolism but also making it difficult to allow lipids to accumulate as triacylglycerols. This series of actions eventually results in development of lowering action for blood remnant-like lipoprotein level and also lowering action for blood leptin level, and hence, lipid metabolism is improved. Further, energy consumption is enhanced by promoting the induction of β-oxidation and activating lipid catabolism.
US20060063753 Use of nefopam for the treatment of nausea or emesis The invention relates to the use of nefopam for the manufacture of a medicament for the treatment of nausea, dizziness, blurred vision and emesis.
US20110082190 Nucleic Acids Encoding Anti-IL-12 Antibody Isolated anti-IL-12 antibodies, nucleic acids encoding antibodies or antibody portions, vectors, host cells, and methods of making are useful for production of antibody or portions for treating and/or diagnosing IL-12 related conditions, diseases, and disorders.
WO2007008539A3 Pyranopyridine compounds The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to a chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell.
CN103585173A Pharmaceutical composition containing sodium sulfate and sodium picosulfate The invention belongs to the field of pharmacy, and relates to a pharmaceutical composition for clearing mammal intestinal tract. The pharmaceutical composition is characterized by comprising: 2 g-15 g of sodium sulfate and 2 mg-20 mg of sodium picosulfate or pharmaceutically acceptable salts thereof.
CN1593454A Magnesium, potassium and calcium mixture and its usage The invention discloses a magnesium, potassium and calcium mixture and its use thereof, characterized in that it is prepared from the following raw materials (by weight parts), magnesium 120-240 parts, potassium 37.5-112.5 parts, calcium 120-240 parts, microelement 15.5-24.5 parts, vitamin 160-220 parts, and folic acid 100-150 parts.
CA2624686A1 Therapeutic molecules and their uses The present invention relates with the identification and use of oligonucleotides acting by a sequence independent mode of action for the prevention and treatment of thrombotic disorders, cholesterol related disorders, dyslipidemia, osteoporosis and snake venom effects.
WO2013082490A1 Substituted anilines as ccr(4) antagonists Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
CN101265248B Cembrene lactone type diterpenoid lobophilides A and B, and preparation method and use thereof The invention relates to cembranolides with formulas of pod flexibilide A and pod flexibilide B extracted and separated from Sinularia polydactyla, preparation method and application thereof. A plurality of in vitro antitumor activity experiments indicate that the cembranolides have obvious tumor cell inhibiting activity, and prospect application in drug for treating caner/tumor. The invention also provides a precursor for the research of new drugs for treating various common multiple cancers. The cembranolides and the preparation method thereof are important to exploitation and utilization ofthe Chinese marine biological resources.
US7541337 Methods and compositions for the treatment of peripheral artery disease Compositions and methods for treating peripheral artery disease in a patient are provided. Compositions comprise recombinant fibroblast growth factor-2. Fibroblast growth factor, such as FGF-2, is administered in therapeutically effective amounts to treat or prevent peripheral artery disease including claudication and critical limb ischemia. Pharmaceutical compositions comprising a therapeutically effective amount of FGF-2 and a pharmaceutically acceptable carrier are also provided. The methods of the invention to treat peripheral artery disease and claudication comprise administering at least a single dose of a pharmaceutical composition comprising the FGF, such as FGF-2, via intra-arterial, intravenous, or intramuscular infusion to the patient. It is recognized that increased benefits may result from multiple dosing, including intermittent dosing.
CN101791346A Preparation method of soft capsule for quitting smoking, relieving alcoholism and cleaning oral cavity The invention provides a preparation method of soft capsule for quitting smoking, relieving alcoholism and cleaning oral cavity; A formulation with effect of quitting smoking contains 15 g of white ginseng, 45 g of polygala root, 65-80 g of white radish, 50 g of cordate houttuynia, 10 g of red jujube, 45 g of earthworm, and 50 g of liquorice; B formulation with effect of relieving alcoholism contains 15 g of radix sophorae flavescentis, 20 g of betelnut pieces, 5 g of ginseng, 20 g of kudzuvine flower, 10 g of Chinese angelica, 15 g of hypericum japonicum thunb, 10 g of rhizoma acori graminei, 12 g of rhizoma pinelliae preparatum, 20 g of fructus alpiniae oxyphyllae, 10 g of szechuan lovage rhizome and 100 g of honey; C formulation with effect of cleaning teeth contains vitamin D, chlorophyll, fluorine, abradant, natural essence and interfacial surfactant; the processing method comprises the following steps: adding 800-100 g of water to the A and B formulations to decoct for 40 min, then filtering the liquid medicine, mixing with the C and D formulations uniformly, decocting as colloidal; taking out to slice, and finally, packing as soft capsule. The soft capsule can be carried about, and can be chewed in the mouth anytime; the invention has the functions of quitting smoking, relieving alcoholism, whitening teeth and cleaning oral cavity, thereby facilitating to protection of human health.
CN1813786A Glycosaminogly can for preparing medicine or dressing for treating or repairing skin wound The present invention relates to application of aminopolysaccharide in preparation of medicine for curing traumata of skin and dressing for protecting and repairing traumata of skin. The described aminopolysaccharide is carboxymethyl chitosan and/or carboxymethyl chitin, and the described traumata of skin include skin burn, scald, dermal ulcer and dermal machine traumata.
WO2013120229A1 METHOD FOR PREPARING AQUEOUS MANO PARTICLE SUSPENSIONS OF DERIVATIVES OF 4,9-DIHYDROXY-NAPHTHO[2,3-b]FURAN ALIPHATIC ACID ESTERS Disclosed is a method for preparing aqueous nanoparticle suspensions of derivatives of 4,9-dihydroxy-naphtho[2,3-b]furan aliphatic acid esters. The compositions and the uses of the aqueous nanoparticle suspensions prepared according to the method as described herein are also disclosed.
WO2006095542A1 Pharmaceutical composition comprising amine compound [PROBLEMS] To improve hygroscopicity and/or stability of an amine compound represented by formula (1). [MEANS FOR SOLVING PROBLEMS] The amine compound is mixed with a complex with cyclodextrin or polyethylene glycol to remarkably improve hygroscopicity and/or stability of a salt of the compound, whereby a solid material which satisfies the requirements needed for use as a pharmaceutical active ingredient (e.g., stability) can be produced.
WO2014092572A1 Improved methods for cancer treatment with a genotoxic agent The invention relates to a susceptibility agent for rise in a method for treatment of an individual suffering from, cancer, whereby said susceptibility agent is combined with a genotoxic agent. Said genotoxic agent is preferably selected from gamma radiation, a. platinum-based compound and/or an anthracyciin, A preferred susceptibility agent inhibits expression and/or activity of a. product of a gene selected from the group consisting of AKIHL DUSP15, UBE1X, RPL7L1, USp8; 4EHP and PRKDL
CN103750308A Composition with effect of improving gastrointestinal functions The invention discloses a composition with the effect of improving gastrointestinal functions. The composition contains following components in parts by weight: 1-4 parts of mannan or gulcomannan, 3-6 parts of prebiotics, 2-5 parts of Chinese yams or 30-60 parts of asparaguses and protein powder. The oral composition is unique in formula and scientific in use ratio and has the advantages of easiness for preparation, low production cost and the like; the oral composition can be prepared into various medicines, foods or health-care foods by using the method which is acceptable in production; the prepared product has the effects of improving diarrhea, astriction, heat gaining, gastrointestinal dysfunctions or intestinal bacilli illness and the like, and also has the effect of improving the immunity.
CN102008434B Compound docetaxel ester microsphere injection and preparation method thereof The invention discloses a compound docetaxel ester microsphere injection and a preparation method thereof, belonging to the technical field of medicines. The compound docetaxel ester microsphere injection is characterized by being prepared from the following raw materials in weight parts: 0.5 to 5 parts of docetaxel, 30-150 parts of Brucea javanica oil, 30-150 parts of middle-chain triglyceride, 10-30 parts of lecithin, 10-60 parts of polyethylene glycol surface active agents, 20-35 parts of glycerine and 700-950 parts of sterilized water for injection. The compound docetaxel ester microsphere injection of the invention is oil in water type microsphere preparation. The docetaxel as a main drug is coated in the Brucea javanica and middle-chain triglyceride compound oil phase of the oil in water type microsphere. The microsphere has a smaller grain diameter (which is lower than 100nm), and the preparation has better stability. The compound oil phase compositions play a cooperative anticancer role, and reduce the stimulation reaction of the injection and the side reactions such as hemolysis, allergy and the like. The invention has targeting function and increases the medicine effect.
CN103099789A Preparation method of vitamin C granules The invention provides a preparation method of vitamin C granules. The method comprises: smashing a vitamin C crystal, then adding an adhesive to prepare them into a soft material, then preparing the soft material into wet granules by a rounding machine, and carrying out drying and sieving treatment, thus finally obtaining the vitamin C granules that can undergo direct tabletting. The preparation method provided in the invention has the advantages of simple steps and low cost, and the prepared vitamin C granules have good fluidity and compression molding performance.
CN102872057A Application of Gypensapogenin A to preparing drugs for treating yellow fever virus infection The invention discloses application of Gypensapogenin A to preparing drugs for treating or preventing yellow fever virus infection. Gypensapogenin A is capable of effectively inhibiting the proliferation of yellow fever virus, has little toxicity to cells, can be further developed as the drugs for treating diseases caused by virus infection and has extensive application prospect. The application of Gypensapogenin A to preparing the drugs for treating the yellow fever virus infection, disclosed by the invention, is firstly published, the framework type is brand new, the activity of inhibiting the yellow fever virus is unexpectedly strong and the probability of giving any revelation by other compounds does not exist, so that prominent substantive features are provided and a remarkable progress in preventing and treating the yellow fever virus infection is made at the same time.
US20110130707 Thiadiazole Compounds and Uses Thereof Thiadiazole compounds, compositions, bioconjugates, and methods for targeting and photoactivation at target sites.
CN102973669A Throat clearing sustained release tablet and preparation method thereof The invention discloses a throat clearing sustained release tablet and a preparation method thereof. The method comprises the following steps of: extracting water from myrobalan, filtering the water, and obtaining paste 1 through concentration; implementing alcohol precipitation, and reclaiming ethanol to obtain myrobalan paste; taking indigo naturalis for dipping in sulfuric acid water solution, washing the indigo naturalis to take a neutral property, and obtaining refined indigo naturalis through drying; adding water in liquorice for extracting and filtering, and obtaining paste 2 through concentration; adding ethanol in the paste 2, stewing, taking supernatant, regulating pH value, filtering, reclaiming the ethanol from filtrate, adding water, regulating pH value, filtering, washing precipitate by the water, and obtaining liquorice extractant through drying; drying and smashing the myrobalan paste, and evenly mixing the smashed myrobalan paste with the smashed refined indigo naturalis, calculus bovis factitius, borneol, menthol and the liquorice extractant to obtain a mixture, screening and evenly mixing the mixture, filling agent, hydroxypropyl methylcellulose and release speed regulator, adding adhesive for producing a soft material, screening and pelletizing, drying, finishing particles and tabletting. The throat clearing sustained release tablet has the advantages of low cost, safety, quick effect, good curative effect, convenience for carrying, few working hours, high transfer rate of effective components and high safety for operators.
EP1809273B1 Use of 2-phenyl-1,2-ethanediol-(di)carbamates for treating epileptogenesis This invention is directed to methods for preventing, treating, reversing, inhibiting or arresting epilepsy and epileptogenesis in a subject comprising administering to the subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II), or a pharmaceutically acceptable salt or ester thereof,: Formula (I) Formula (II) wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).
EP2785709A1 Aminopyrimidine derivatives as lrrk2 modulators Compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
EP2268291A2 Treatment for the hair regrowth in the bald patches formed by alopecia of the celsi area The aim of present invention is to provide a procedure, a technique and a product able to induce the hair regrowth in the bald patches which have formed because of alopecia. Such a technique, does not have the disadvantages of the classic hair transplant. A further aim of the invention is that of providing a method with which it is possible to have new growth of hair on the bald patches on humans the use of the product. Furthermore, the aim is to provide a relatively simple method of application. The above aims can be reached by using the method based on the invention so that the hair grows again naturally. The invention, therefore, refers to the regrowth of hair, in alopecia.
WO2012078980A2 Compositions, methods and kits for remineralization and inhibition of dental caries in teeth Methods, compositions and kits are provided for enhancing remineralization of a tooth or bone containing hydroxyapatite and inhibiting caries progression or loss of hydroxyapatite using a bisphosphonate or pyrophosphonate. The tooth or tooth surface contains a trauma or defect, for example the tooth contains a caries that is identified using a detectable probe. The bisphosphonate or pyrophosphonate is contacted to the tooth and/or oral cavity and binds to the hydroxyapatite material in the tooth or bone and prevents loss of hydroxyapatite material or strengthens the hydroxyapatite. The amount and extent of enhanced remineralization or of inhibition of caries progression and loss of hydroxyapatite are determined by techniques including photography, light microscopy and fluorescence microscopy.
CN1864665B Method for preparation of drug-encapsulating polymer micelle The provided preparation method for macromolecular micelle contained drug inside comprises: (A) preparing the aqueous dispersion liquid with block copolymer of hydrophilic chain and hydrophobic or charged chain; (B) preparing the fatsoluble drug by organic solvent without mixing with water; (C) mixing, stirring, volatilizing solvent, and preparing the final product.
CN103202834A Applications of oridonin in the preparation of antineoplastic drugs The invention belongs to the fields of chemical and pharmaceutical, relating to applications of oridonin in the preparation of antineoplastic drugs. The present invention provides applications of oridonin in the preparation of antineoplastic drugs; wherein the tumor cells include liver cancer cells, lung adenocarcinoma cells and pancreatic cancer cells. The oridonin is a natural product of low toxicity, high bioavailability and stable nature, and has clinical value. As a new antineoplastic drug or an auxiliary component for antineoplastic drugs for development, the small molecule compound of this invention has an obvious tumor suppression effect and is environment protecting, providing a new way and method for treating and curing tumours.
WO2012075210A3 Method for treating refractory cancer Therapeutic methods for treating refractory cancers are disclosed comprising administering to a patient in need of treatment a compound of Formula (I) disclosed herein.
CN101870692A Novel piperazinyl pyridazine compounds The invention relates to novel piperazinyl pyridazine compounds in a formula I or salts thereof, a preparation method thereof and use thereof as nervous inflammation inhibitors in treating or preventing neurodegenerative diseases such as senile dementia, Parkinson's disease, cognitive impairment and the like or treating diseases such as mental disorder, epilepsy, convulsions, stroke and the like. The compounds have the advantages of simple preparation process, readily available raw materials and suitability for industrial large-scale production. In addition, through the verification of in-vitro experiments, the compounds have the effect of inhibiting BV2 from secreting IL-1 beta efficiently, and the effect is superior to that of positive medicaments; and simultaneously, the compound have no inhibiting effect on the secretion of the IL-1 beta by C6, and thus the compounds have high safety.
US7267977 Peripheral-type benzodiazepine receptor: a tool for detection, diagnosis, prognosis, and treatment of cancer The expression and subcellular localization of peripheral-type benzodiazepine receptors (PBR) is shown in this application to correlate with the metastatic potential of cells, and increased cell proliferation. Inhibition of PBR expression, function or stability results in a decrease in cell proliferation. Compositions and methods for regulating and/or monitoring PBR and its expression are useful for the detection, diagnosis, prognosis and treatment of solid tumors, in particular, breast cancer.
EP1583525B1 Use of porphyrin synthesis substances in combination with salicylates and antioxidants for use in phototherapy to cure skin and articulation diseases The invention relates to the use of porphyrin synthesis substances, in particular 5-amonolevulinic acid, if necessary in combination with salicylates in the form of acetylsalicyc acid and with antioxydising agents in the form of ascorbic acid when a phototherapy is carried out with a light emission whose wavelength ranges from 400 to 700 nm pour treating inflammatory processes, for instance on the skin and/or articulations of mammalians and human beings, in particular for curing arthritis, simple psoriasis, arthopathic psoriasis and neuropathies such as a carpal tunnel syndrome or Bechterev's disease.
CN1981772A Composition and method for decreasing concentration of low density lipoprotein cholesterol A composition for decreasing low-density lipoprotein (LDL) and cholesterol contains vegetative sterol, soybean protein and/or isoflavone. A method for decreasing the contents of LDL and cholesterol in human blood and a method for preventing or relaxing atherosclerosis are also disclosed, which feature that said composition is orally taken.
WO2014031584A1 Haptens of aripiprazole and their use in immunoassays The invention relates to compounds of Formula I, wherein R1, R2, and R3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from aripiprazole. The invention also relates to conjugates of an aripiprazole hapten and a protein.
US20110201578 Composition and methods for the treatment of pseudofolliculitis barbae and skin irritation The invention comprises a composition for the treatment of pseudofolliculitis barbae and a method of use therefor. Preferred embodiments include compositions containing one or more of active ingredients L-arginine, acetylsalicyclic acid, and salicyclic acid adjusted to a pH in the range of 4.0 to 6.0. Preferred compositions include: a carrier, such as water; a moisturizer, such as propylene glycol, and one or more of the active ingredients. Application of a composition for the treatment of pseudofolliculitis barbae with a pH of about skin does not disrupt normal skin functioning.
WO2005080384A2 Benzimidazole derivative and use as aii receptor antagonist The present invention relates to a compound represented by the formula (I) wherein R1 is a group represented by the formula wherein R2, R3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or a C6 - 1 alkyl, or a salt thereof. The compound of the present invention is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and metabolic diseases such as diabetes and the like.
EP2134345A2 Triazolquinolonic derivatives with antimycobacterial activity The use of triazoloquinolone derivatives in the production of a drug useful for the treatment of diseases caused by Mycobacterium is described. New compounds have been designed and synthesised, which have manifested a high level of activity vis-a-vis various strains of clinical interest. Said compounds are useful for the formulation of appropriate pharmaceutical compositions for the use of new broad-spectrum drugs.
US20120029060 Antisense Oligonucleotides for Inducing Exon Skipping and Methods of Use Thereof An antisense molecule capable of binding to a selected target site to induce exon skipping in the dystrophin gene, as set forth in SEQ ID NO: 1 to 202.
WO2013172297A1 Preparation containing 6,7-unsaturated-7-carbamoylmorphinan derivative Provided is a solid preparation in which the elutability and stability of a 6,7-unsaturated-7-carbamoylmorphinan derivative is improved. A solid preparation or a coated solid preparation, which comprises a 6,7-unsaturated-7-carbamoylmorphinan derivative, croscarmellose sodium and iron oxide and does not contain titanium oxide, can have an elution ratio of 85% or more 15 minutes after the start of an elution test and can also have improved stability, particularly photostability.
US20080058412 1-(4-((R,S)-5-[1,2]dithiolan-3-ylpentyloxy)-3,5-dimethylphenyl)-3-(4-carboxydimethylmethyloxy-3,5-dimethylphenyl)prop-2-en-1-one; peroxisome proliferator activated receptor agonist; lipid or glucose metabolism: hyperlipidemia, diabetes, obesity; dermatologicalal: psoriasis, atopic dermatitis, acne The invention relates to substituted 1,3-diphenylprop-2-en-1-one derivative compounds, pharmaceutical and/or cosmetic compositions containing same, and the applications thereof in therapeutics and cosmetics. The invention also relates to a method for preparing said derivatives.
CN101890055A Medicinal composition with anti-fatigue effect The invention belongs to the technical field of medicines or foods, and discloses a medicinal composition which contains fermented cordyceps fungal powder and D-ribose, and is characterized by comprising 100 to 500 weight parts of fermented cordyceps fungal powder and 1 to 200 weight parts of D-ribose. Pharmacology experiments show that the medicinal composition has good anti-fatigue effect.
CN103385885A Carbohydrate inhibitor used for treating diabetes The invention relates to a carbohydrate inhibitor selectively inhibiting alpha-glucosidase. The inhibitor has positive charge and stereoisomerism. The inhibitor has high activity, and can be used for treating diabetes.
US20080021038 Novel Piperidine/8-Azabicyclo [3.2.1.] Octan Derivatives As Modulators Of Chemokine Receptor Ccr5 Compounds of formula (I) wherein neither R4 nor R5 is hydrogen; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
US20080242643 4-[({[4,5-bis(nitrooxy)pentyl]oxy}carbonyl)oxy]-3-[4-(methylsulfonyl)phenyl]-2-phenylbut-2-enoic acid; antiinflammatory, analgesic agent; rheumatic diseases, influenza, common cold, pain, dysmenorrhea, headache, neuralgia, synovitis, arthritis, osteoarthritis, cardiovascular disorders, anticoagulants The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. Formula (I). The invention also encompasses certain pharmaceutical compositions and methods for treating cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula 1. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while also reducing the risk of thrombotic cardiovascular events.
US20080085318 Coated compositions and methods for preparing same The present invention provides methods for preparing a coated pharmaceutical composition comprising the steps of a) providing a pharmaceutically active agent or a nutraceutical; b) providing a solution or a dispersion of a polyvinyl-based, cellulose-based, acrylate-based, or shellac polymeric coating composition, and mixtures thereof, in a solvent selected from the group consisting of C1-C3 alcohols, acetone, and ethyl acetate; and c) coating the pharmaceutical active agent or nutraceutical from step (a) with the coating composition from step (b) in a fluid bed processor by spraying the coating solution from a top spray position downwardly onto the pharmaceutical active agent or nutraceutical to provide the coated pharmaceutical composition. The polymer from the coating composition is present in the coated pharmaceutical composition in an amount from about 1% w/w to about 15% w/w on a dry weight basis.
CN101002732A Germ-free medicinal compsns. An aseptic medicinal composition, especially the one containing medicines and EDTA salt, is disclosed.
CN103435619A Pochonicine analogue or pharmaceutically acceptable salts of pochonicine analogue and application of pochonicine analogue or pharmaceutically acceptable salts of pochonicine analogue The invention discloses a pochonicine analogue or pharmaceutically acceptable salts of the pochonicine analogue. The pochonicine analogue can be a compound shown in the formula 1, the formula 2 or the formula 3, wherein the pochonicine analogue or the pharmaceutically acceptable salts of the pochonicine analogue have good inhibitory activity to various enzymes. Thus, the pochonicine analogue can be used as a glycosidase inhibitor and also can be applied to preparation of medicaments and pesticides.
WO2006034113A2 Quinolone analogs as cell proliferation inhibitors The present invention provides quinolone analogs of formula (I) which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing quinolone analogs, and methods of using the same.
CN101019872B Nanometer antiviral liposome medicine and its preparation The present invention relates to one kind of nanometer antiviral liposome medicine and its preparation process. The nanometer antiviral liposome medicine includes the mixture of alprostadil and Adefovir dipivoxil in the weight ratio of 0.1-1.0 to 50-300 in 10.1-80.2 weight portions, soybean lecithin 88-440 weight portions, the mixture of cholesterol and soyasterol in the weight ratio of 9 to 1 in40-200 weight portions, the mixture of polyglycol-4000 and polyglycol-2000 in the same ratio in 15-40 weight portions, sodium glucuronate in 100-280 weight portions, vitamin C in 160-800 and glutathione in 5-10 weight portions. The nanometer antiviral liposome medicine is used as the broad spectrum antiviral medicine.
EP1307205B1 Use of 7alpha-hydroxy-estradiol, 7alpha-hydroxy-dehydroepiandrosterone and 7alpha-hydroxy-pregnenolone derivatives for treating acute cellular degeneration A method is provided for treating a patient in need of therapy for acute neuronal degeneration due to metabolic compromise of central or peripheral nervous system cells comprising administering to that patient a therapeutically effective amount of a 7α-hydroxy substituted steroid selected from 7α-hydroxy-derivatives of estradiols, dehydroepiandrosterones and pregnenolones, and metabolic precursors thereof. Use of such compounds for manufacture of medicaments and neuroprotective compositions are also provided.
WO2014038630A1 Cesium-excreting agent, poisonous metal-excreting agent, food or beverage, feed, and medicinal product Provided are: a cesium-excreting agent and a poisonous metal-excreting agent which can suppress the absorption of cesium or a poisonous metal into the body or can promote the excretion of cesium or a poisonous metal out of the body; and a food or beverage, a feed and a medicinal product. A cesium-excreting agent and a poisonous metal-excreting agent, each of which comprises calcium alginate as an active ingredient; and a food or beverage, a feed and a medicinal product, each of which contains the cesium-excreting agent or the poisonous metal-excreting agent.
CN1839839A Preparation method of ziprasidone or its salt inclusion The invention relates to a process for preparing Ziprasidone or its salt inclusion compound, which comprises the steps of, (1) providing a solution of Ziprasidone or its salts, heating the solution at 78+-1.5 deg C to dissolve Ziprasidone or its salts, (2) filtering non-soluble substance in the solution, then drying the dissolvent.
US7514442 Trisubstituted 4-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
WO2007017546A3 Method of obtaining tryptamine derivatives The invention relates to a method of obtaining tryptamine derivatives (I), wherein R is a radical of a heterocycle, comprising the decarboxylation of the corresponding derivative of 3-(2-aminoethyl)-1H-indole carboxylic acid and the subsequent methylation of the amino group. Compounds (I) include zolmitriptan and rizatriptan which can be used for the treatment of migraines.
WO2010107984A1 Novel alpha-(n-sulfonamido)acetamide compounds incorporating deuterium as inhibitors of beta amyloid peptide production a novel alpha-(n-sulfonamido) acetamide compound incorporating deuterium as inhibitor of beta amyloid peptide production The present disclosure provides novel deuterated alpha-(N-sulfonamido)acetamide compounds, their pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease, head trauma, traumatic brain injury, and/or dementia pugilistica and/or other conditions associated with β-amyloid peptide.
CN1759826A Coating method for microcapsule of lysine hydrochloride A method for coating on the surface of lysine hydrochloride microsoftgel includes such steps as providing stearic acid as the coating material, loading lysine hydrochloride particles in a coating chamber, forcing the compressed air to flow upward, driving the lysine hydrochloride particles to be suspended in flowable state, and spraying said coating material on the surface of each lysine hydrochloride particle.
CN101496832A Externally-applied medicament for treating cervical erosion and preparation method thereof The invention relates to an externally applied medicine for treating cervical erosion, which mainly takes swine gall bladder, alum, elephant hide and kuh-seng as raw materials. The raw materials are washed to be clean, smashed, dried and crushed into 80-100 mesh fine powder which is externally applied to erosive cervix uteri. The externally applied medicine has the advantages of low dosage, short treatment period, high cure rate, low treatment cost, simple treatment method and the like.
WO2014067499A1 Stabilization of tiotropium solvates A method for stabilization of micronized or milled solvates of tiotropium bromide, in which the solvates are deposited in a saturated atmosphere of the adequate solvent for the time period sufficient for recovery of the original amount of solvent in the solvate. A stable tiotropium bromide solvate with 1,3-propanediol.
WO2010011548A1 Novel substituted sulfamide derivatives The present invention is directed to novel substituted sulfamide derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives form in the treatment of anxiety and related disorders; bipolar depression and mania; depression; epilepsy and related disorders; epileptogenesis; glucose related disorders; lipid related disorders; migraine; obesity; pain; substance abuse and as neuroprotective agents. The present invention is further directed to a process for the preparation of the novel substituted sulfamide derivatives.
EP1730111A2 Substituted bisarylurea derivatives as kinase inhibitors The present invention relates to bisarylurea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
CN101849962A Lipid-lowering and weight-losing complex nutrient preparation and preparation method thereof The invention discloses a lipid-lowering and weight-losing complex nutrient preparation and a preparation method thereof. The preparation is prepared with the following raw materials by molar ratio: conjugated linoleic acid, soluble zinc salt, soluble ferrous salt, soluble magnesium salt and soluble calcium salt, with the molar ratio being 200: (0.35-0.65): (0.65-1.5): (20-50): (50-100). The preparation method comprises the following steps: carrying out saponifiacation reaction of the conjugated linoleic acid with a biological functional activity and aqueous solution or alcoholic solution of alkali metal hydroxides or alkali metal alcoholate at the room temperature or a temperature close to the room temperature under the inert gas protection, and synthesis reaction of the reaction products with metal salt solution of soluble nutrient elements, thereby obtaining the lipid-lowering and weight-losing complex nutrient preparation. The invention has the advantages of simple process and easy operation, and the preparation product has the advantages of high purity and stable quality, and can be used as the functional additive, pharmaceutical component and feed additive of the nutrient.
EP2109613A2 Polymorphs of eszopiclone malate The present invention provides crystalline Eszopiclone malate form II, crystalline Eszopiclone form V, processes from preparing the crystalline Eszopiclone malate form II or V, pharmaceutical compositions comprising the crystalline Eszopiclone malate form II or V and methods of treating insomnia comprising administering the crystalline Eszopiclone malate form II or V.
US20110244044 Compound, medicament, vaccine composition and nanocapsules The present invention relates to a compound comprising a polyelectrolyte and, covalently linked thereto, an immunological adjuvant and/or cell targeting ligand, wherein the covalently linked entity can have both adjuvant and cell targeting characteristics. The compound is used in the preparation of hydrophilic vaccine nanoparticles, which preferably have an antigenic compound or therapeutic agent, or genetic information encoding such compounds or agents entrapped in their matrix, or covalently linked to their surfaces. Vaccine compositions comprising the particles of the invention are advantageous, because a strong and long-lasting immune response is obtained following administration of a single dose. In a preferred embodiment, the polyelectrolyte of the compound is an anionic polymer, and the particle comprises a matrix comprising chitosan.
US20050154026 Suitable for the treatment of gastric and intestinal disorders; in particular, omeprazole, rabeprazole, pantoprazole, esomeprazole The invention relates to the use of proton pump inhibitors in the treatment of non-cardiac chest pain.
US20050124586 Alpha-substituted arylalkyl phosphonate derivatives The present invention relates to novel α-substituted arylalkylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.
WO2010004339A1 Processes for the preparation of crystalline forms of sunitinib malate The present invention, relates to novel processes for the preparation of sunitinib malate formula (I), pharmaceutical compositions comprising said polymorph and the use of the said pharmaceutical compositions in the treatment of various forms of cancer.
CN102018907A Medicine for treating fever in children and preparation method thereof The invention discloses a medicine for treating fever in children, which is mainly prepared from the following medicinal materials based on a fixed weight ratio: gypsum, rhizoma anemarrhenae, sweet wormwood, tree peony bark and the like. The medicine has the action on clearing away heat and toxic material, nourishing Yin and moistening dryness, cooling blood and purging intense heat, and has high speed of taking effect, good curative effect and high cure rate for treating fever in children.
CN103347511A Potentiator of antitumor activity of chemotherapeutic agent The invention relates to an agent for potentiating the antitumor activity of a chemotherapeutic agent for cancer including cancer stem cells, comprising at least one branched-chain amino acid selected from isoleucine, leucine, and valine or a salt thereof. The invention also relates to an agent for treating cancer including cancer stem cells, comprising at least one branched-chain amino acid selected from isoleucine, leucine, and valine or a salt thereof, and a chemotherapeutic agent in combination. The invention also relates to an agent for preventing the metastasis or recurrence of cancer including cancer stem cells, comprising at least one branched-chain amino acid selected from isoleucine, leucine, and valine or a salt thereof, and a chemotherapeutic agent in combination.
CN102048702B Bifendate nano crystal preparation and preparation method thereof The invention discloses a bifendate nano crystal preparation, which comprises 200 weight parts of raw material of bifendate and 20 to 400 weight parts of auxiliary material of stabilizing agent. A preparation method comprises the following steps of: (1) dispersing the stabilizing agent serving as a dispersion medium in double distilled water to obtain a suspension A; (2) dispersing the bifendate in an organic solvent to obtain a coarse suspension B; (3) dispersing the coarse suspension B in the suspension A under the ultrasonic condition to obtain a suspension C; (4) homogenizing the suspension C by using a high pressure microfluidization nano dispersion instrument to obtain bifendate nano crystal suspension; and (5) performing freeze drying on the prepared bifendate nano crystal suspension, or adding a freeze drying protective agent and performing freeze drying to obtain the bifendate nano crystal preparation. The bifendate nano crystal preparation can be prepared into injection or oral preparations such as tablets, capsules and the like when applied.
CN102166283A Externally-applied treatment fluid for treating burns and scalds and preparation method thereof The invention relates to an externally-applied treatment fluid and a preparation method thereof, in particular to an externally-applied treatment fluid for treating burns and scalds and a preparation method thereof, belonging to medical medicines for external use. The externally-applied treatment fluid provided by the invention for treating burns and scalds comprises the following ingredients in parts by weight: 5-15 parts of giant knotweed, 10-20 parts of pubescent holly root, 1-2 parts of cicada slough, 40-60 parts of Rhaphiolepis indica bark, 4-12 parts of corydalis tuber, 10-20 parts of common jujube bark, 5-15 parts of golden thread, 10-20 parts of shore podgrass all-grass root, 10-25 parts of Rubus pectinellus bark, 10-25 parts of Cibolium Baromelz bark, 10-20 parts of peach tree root, 10-25 parts of camphor tree root and 120-200 parts of white spirit (with the alcoholic content of 60%). During usage, the product of the treatment liquid provided by the invention is applied to surfaces of the scalds and then applied again when the surfaces of the scalds begin to become dry; under a situation that the scald surfaces are kept in a wet state, 2-12 or even more applications are needed every day; the pain can be killed after several minutes; a treatment effect can be obtained after 1-2 days; and generally, the scalds can be scabbed and healed within seven days. For purulent wounds or wounds that cannot be healed for a long time, higher usage level of the product is needed and the use frequency is increased.
CN103520147A Application of puerarin or medicinal composition containing puerarin in preparation of medicament with effect of preventing or treating senile dementia The invention discloses application of puerarin or a medicinal composition containing the puerarin in preparation of a medicament with an effect of preventing or treating senile dementia. The puerarin can be singly used as a medicament or can be used together with other senile dementia medicaments with different mechanisms of action when used for treating or preventing the senile dementia of people or mammals, wherein the puerarin not only can reduce side or toxic effects of medicaments but also can achieve an effective of collaborative treatment when used for treating the senile dementia together with a medicinal composition consisting of triptolide, galantamine and borneol. The puerarin can significantly inhibit the deposition of beta-amyloid, and has a definite curative effect and small side effects when used for preventing and treating the senile dementia, so that the puerarin has a wide medical application prospect.
CN101264079A Oxymatrine nano preparations for liver cell targeting injection and preparation thereof The invention relates to medicine preparation field in particular to hepatocyte targeting oxymatrine nanometer powder injection and the preparation method for the treatment of hepatitis b, severe hepatitis and severe jaundice hepatitis. The invention is characterized in that the oxymatrine nanometer powder injection comprises oxymatrine, stearic acid, lecithin for injection, glycyrrhetinic acid, surfacetant and frozen dried adjunct. After dissolution and heating, the organic phase is formed; the solvent is agitated and evaporated in the heating condition to get the colloidal solution; then after agitating and filtering, the even nanometer grade dispersion; after the frozen dried adjunct is added, the mixing ultrasounding and frozen storage is made; according to the preparation course method, the discharging of medicine is reduced; the time that the oxymatrine stay in the body is prolonged; the medicine tends to and is centralized to the liver; therefore, the therapeutic effect is improved. The invention has the advantages that the preparation is simple; the sustained release effect is obvious; the time that the medicine staying in the body is raised; the liver forward effect is excellent; the therapeutic effect is outstanding.
US6977264 For therapy and prophylaxis of obesity, diabetes Selected substituted piperidine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
CN103160557A Purpose of ribosomal protein S5 in catalyzing of protein molecules for generatation of dephosphorylation reaction The invention provides a purpose of ribosomal protein S5 (RPS5) in catalyzing of protein molecules for generation of dephosphorylation reaction, the ribosomal protein S5 serves as PP2C sampling protein phosphatase, provides purposes of RPS5 or agonist or inhibitor of the RPS5, the RPS5 or the agonist or the inhibitor of the RPS5 is used for preparing compounds for treating diseases or a pathological process which an Akt and MAPK access participates in, and further provides a detection method of the RPS5 protein phosphatase activity and a method for screening the agonist or the inhibitor of the RPS5. The invention has the advantages that the RPS5 is demonstrated to be the PP2C sampling protein phosphatase for the first time, the Akt and MAPK access is regulated and controlled, and therefore the RPS5 self can be used as the protein phosphatase, can be used for preparing the compounds for treating the diseases or the pathological process which the Akt and MAPK access participates in or screening substances restraining or activating the RPS5, and is used for treating the diseases or the pathological process which the Akt and MAPK access participates in.
US20120322719 Methods of treatment of fatty liver disease by pharmacological activation of cholinergic pathways A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.
US20100226855 Rate-Controlled Oral Dosage Formulations The present invention relates to a drug delivery system, in which a drug containing core, either alone or coated with a rate controlling membrane system, is enveloped on its circumference by an optionally bioadhesive coating, thereby yielding a monolithic system that allows for drug release in a regulated manner.
US7192979 EP4 receptor selective agonist in the treatment of osteoporosis This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, wherein R2, X, Z and Q are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds. This invention is also directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth in a mammal comprising administering those compounds.
CA2311530C Nasal solutions The invention relates to liquid pharmaceutical compositions adapted to nasal administration. The liquid nasal formulations of the invention are characterized inter alia by having excellent and prolonged moisturizing properties.
CA2102494C A pharmaceutical composition containing a defined lipid system The present invention relates to pharmaceutical compositions containing a defined lipid system of at least two lipid com-ponents where at least one of the lipid components is amphiphatic and polar and one is nonpolar wherein the pharmaceutically active compound is a heparin or a fragment therof. In the compositions a water containing solvent also is included in such an amount that discrete lipid particles are present, and said compositions can be adapted to various administration forms such as rectal, oral, buccal, transdermal, etc.
US20090226540 Methods and Compositions For Treating Feline Hyperthyroidism Methods for treating feline hyperthyroidism comprising (1) administering to a feline an antithyroid agent in conjunction with feeding the feline a composition comprising from about 0.1 to less than about 1 mg/kg iodine or (2) feeding the feline a composition comprising from about 0.1 to less than about 1 mg/kg selenium on a dry matter basis.
EP1829538A1 Solid preparation comprising reduced coenzyme q10 and process for production of the same The present invention has its object to provide a solid preparation containing reduced coenzyme Q10 with high stability by protecting reduced coenzyme Q10 against oxidization to oxidized coenzyme Q10 by molecular oxygen. The present invention provides a solid preparation containing reduced coenzyme Q10 which comprises a solid composition containing reduced coenzyme Q10 coated with at least one coating medium selected from among oil-soluble coating media and water-soluble coating media. The present invention also provides a method for stabilizing a solid preparation containing reduced coenzyme Q10, wherein a solid composition containing reduced coenzyme Q10 is coated with at least one coating medium selected from among oil-soluble coating media and water-soluble coating media to thereby stabilize the resulting solid preparation containing reduced coenzyme Q10.
US20110230451 Identification and use of compounds that affect the fidelity of eukaryotic translation initiation codon selection A screening method for identifying compounds that alter the fidelity with which the initiation codon in mRNAs is recognized by the translational apparatus in eukaryotes is disclosed. This screening method was used to identify compounds having such activity. Methods of altering the fidelity of initiation codon selection are also disclosed. Methods of treating disorders characterized by single nucleotide mutations in initiation codons using compounds identified by the screening method, as well as methods of treating fungal and parasitic infections and hyperproliferative disorders using compounds identified by the screening method are also disclosed.
US20120276217 Disinfecting formulation The present invention provides a disinfecting formulation useful, for example, for cleaning and disinfecting human or animal body parts, and in particular for disinfecting human hands. Typically, the formulation comprises alcohol, one or more essential oils comprising cineole, gelling agent and water. The invention also provides methods of disinfection of human and animal body parts and methods for preparing the formulation.
US20090325960 Method for treating inflammatory diseases using rho kinase inhibitor compounds This invention is directed to methods of preventing or treating diseases or conditions associated with excessive cell proliferation, remodeling, edema and inflammation. Particularly, this invention is directed to methods of treating inflammatory diseases or conditions such as rheumatoid arthritis and inflammatory bowel disease. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a compound of a novel rho kinase inhibitor compound to treat the disease.
CA2654839A1 Use of enoxaparin for reducing the risk of death in acutely ill medical patients The invention relates to the use of enoxaparin for reducing the risk of death in acutely ill medical patients.
EP2157081A1 Indolinones substituted in six locations, their manufacture and their application as medicine 6-Carboxy-3-(anilino- or cycloalkylamino-methylene)-indolin-2-one or -thione derivatives (I) are new. 6-Carboxy-3-(anilino- or cycloalkylamino-methylene)-indolin-2-one or -thione derivatives of formula (I) and their tautomers, diastereomers, enantiomers (and mixtures) and salts are new. [Image] X : O or S; R 1H or prodrug residue; R 2COOH, (1-6C) alkoxycarbonyl (optionally substituted (os) terminally by Ph, heteroaryl, COOH, alkoxycarbonyl, CONH 2, mono- or dialkylaminocarbonyl or (in the case of (2-6C) alkoxycarbonyl) Cl, OH, alkoxy, NH 2 or mono- or dialkylamino), (5-7C) cycloalkoxycarbonyl, arylalkoxycarbonyl, CONH 2, CONHMe or ethylaminocarbonyl (os in the 2-position by OH or alkoxy); or di-(1-2C alkyl)-aminocarbonyl if R 4 is other than aminosulfonylphenyl or N-(1-5C alkyl)-alkylaminocarbonylphenyl; R 3H, 1-6C alkyl, 3-7C cycloalkyl, CF 3 or heteroaryl; or phenyl or naphthyl (both os by 1 or 2 of halo, CF 3, alkyl or alkoxy, and further os by OH, hydroxyalkyl, alkoxyalkyl, CN, carboxyalkyl, alkoxycarbonyl, CONH 2, mono- or dialkylaminocarbonyl, NO 2, NH 2, mono- or dialkylamino, aminoalkyl, alkylcarbonylamino, N-(alkyl)-alkylcarbonylamino, alkylcarbonylaminoalkyl, N-(alkyl)-alkylcarbonylaminoalkyl, alkylsulfonylamino, alkylsulfonylaminoalkyl, N-(alkyl)-alkylsulfonylamino, N-(alkyl)-alkylsulfonylaminoalkyl, arylalkylaminosulfonyl, 4-7C cycloalkylamino, Q, Q-CO-, Q-SO 2-, Q-alkyl-, Q-CO-alkyl-, Q-SO 2-alkyl-, heteroaryl or heteroarylalkyl); Q : 4-7 membered cycloalkyleneimino (CAI), where CH 2 in the 4-position of 6- or 7-membered CAI is optionally replaced by O, S, SO, SO 2, NH or N(alkyl); R 43-7C cycloalkyl (in which the CH 2 in the 4-position of 6-7 membered cycloalkyl is os by NH 2 or mono- or dialkylamino or replaced by NH or N(alkyl)); or phenyl substituted by R 6 and further os by 1 or 2 of halo, 1-5C alkyl, CF 3, alkoxy, COOH, alkoxycarbonyl, NH 2, NHCOMe, alkylsulfonylamino, CONH 2, mono- or dialkylaminocarbonyl, SO 2NH 2, mono- or dialkylaminosulfonyl, NO 2 or CN; R 6e.g. (i) H, halo, CN, NO 2, 1-5C alkyl, 3-7C cycloalkyl, CF 3, heteroaryl, 2,4-dioxo-imidazolidin-5-ylide nemethyl (os by alkyl on either or both N), alkoxy, alkoxyalkoxy, phenylalkoxy, amino-(2-3C) alkoxy, mono- or dialkylamino-(2-3C) alkoxy, phenylalkylamino-(2-3C) alkoxy, N-(alkyl)-phenylalkylamino-( 2-3C) alkoxy, 5-7 membered CAI-(2-3C) alkoxy, alkylthio, COOH, (1-4C) alkoxycarbonyl, CONH 2, alkylaminocarbonyl, N-(1-5C alkyl)-alkylaminocarbonyl, phenylalkylaminocarbonyl, N-(alkyl)-phenylalkylaminocarbonyl, piperazinocarbonyl or N-(alkyl)-piperazinocarbonyl; (ii) alkylaminocarbonyl or N-(1-5C alkyl)-alkylaminocarbonyl, in which an alkyl group is substituted by COOH or alkoxycarbonyl or in the 2- or 3-position by di-(2-3C alkyl)-amino, piperazino, N-alkylpiperazino or 4-7 membered CAI; (iii) (3-7C) cycloalkylcarbonyl (in which the CH 2 in the 4-position of 6-7 membered cycloalkyl is os by NH 2 or mono- or dialkylamino or replaced by NH or N(alkyl)) or (iv) 4-7 membered CAI (in which (a) CH 2 groups bonded to the imino can be replaced by CO or SO 2, (b) the cycloalkylene part is optionally fused with phenyl, (c) 1 or 2 H can be replaced by alkyl and (d) CH 2 in the 4-position of 6- or 7-membered CAI is os by COOH, alkoxycarbonyl, CONH 2, mono- or dialkylaminocarbonyl, phenylalkylamino or N-(alkyl)-phenylalkylamino or replaced by O, S, SO, SO 2, NH, N(alkyl), N(Ph), N(alkanoyl) or N(benzoyl)); R 7e.g. (i) 3-7C cycloalkyl (in which the CH 2 in the 4-position of 6-7 membered cycloalkyl is os by NH 2 or mono- or dialkylamino or replaced by NH or N(alkyl); or in 5-7 membered cycloalkyl (CH 2) 2 is optionally replaced by CONH, (CH 2) 3 is optionally replaced by NHCONH or CONHCO or (CH 2) 4 is optionally replaced by NHCONHCO, where all N atoms are os by alkyl), or (ii) aryl, heteroaryl, OH, alkoxy, NH 2, mono- or di-(1-7C alkyl)-amino, NHPh, N-(phenyl)-alkylamino, phenylalkylamino, N-(alkyl)-phenylalkylamino, di-(phenylalkyl)-amino, mono- or di-(omega -hydroxy-(2-3C) alkyl)-amino, mono- or di-(omega -hydroxy-(2-3C) alkyl)-amino, di-(omega -alkoxy-(2-3C) alkyl)-amino, N-(dioxolan-2-yl)-alkylamino, alkylcarbonylamino-(2-3C) alkylamino, alkylcarbonylamino-(2-3C) alkyl-N-(alkyl)-amino, alkylsulfonylamino, N-(alkyl)-alkylsulfonylamino, alkylsulfonylamino-(2-3C) alkylamino, alkylsulfonylamino-(2-3C) alkyl-N-(alkyl)-amino, carboxyalkylamino, N-(alkyl)-carboxyalkylamino or guanidino (os by 1 or 2 alkyl) and R 5H or alkyl. See DEFINITIONS for 'Full definitions'. An independent claim is included for the preparation of (I). - ACTIVITY : Cytostatic; antirheumatic; antiarthritic; antipsoriatic; ophthalmological; antidiabetic; anti-HIV; nephrotropic; hepatotropic; neuroprotective; antiinflammatory; immunosuppressive; vasotropic; antiarteriosclerotic. - MECHANISM OF ACTION : Kinase inhibitor; receptor tyrosine kinase inhibitor; cyclin dependent kinase complex inhibitor; viral cyclin inhibitor. 3-(Z)-(1-(4-(N-(3-dimethylaminopropyl)-N-acetylamino)-anilino)-1-phen yl-methylene)-6-ethoxycarbonyl-2-indolinone (Ia) exhibited an IC 50 value of 0.003 mu M for inhibition of proliferation of human umbilical endothelial cells.
CA2362858C Compositions and methods for their preparation from lepidium The invention relates to compositions that can be isolated from Lepidium plant material and to methods for their isolation. The compositions are useful for treating and preventing cancer and sexual dysfunction.
CA2153604C Formulations containing esculoside and the use thereof in the pharmaceutical and cosmetic fields The present invention relates to the use of esculoside alone or in combination with adenylate cyclase stimulators, such as forskolin or Salvia miltiorrhiza diterpenes and/or with phosphodiesterase inhibitors, such as apigenine-skeleton dimeric flavones, in topical formulations for the treatment of peripheral vasculopathies related to an impaired peripheral microcirculation, cellulitis or unesthetisms connected with a deposit of superfluous fat. For the reduction of the deposits of superfluous fat of any origin, the above mentioned products are advantageously also combined with caffeine, theophylline and derivatives thereof.
CN102008611A External cream for treating summer-damp cold by using transdermal absorption technology The invention relates to an external cream for treating summer-damp cold by using a transdermal absorption technology, belonging to externally applied drugs. Raw tuber pinellia, tuckahoe, elsholtzia, dried orange peel, Mangnolia officinalis and other Chinese drugs are extracted, and then extracts are mixed with pennyroyal, patchouli oil, alcohol and the like as well as vaseline and other cream substrates to obtain the external cream. In the invention, the transdermal absorption technology is adopted; when in use, the cream is spread on the forehead, temples or oxters of a child patient; the cream has the functions of physically cooling, eliminating dampness and heat, relieving exterior syndrome and removing heat; and by taking effect on both inside and outside of the human body, the cream can treat both the symptoms and root causes of the disease, and has obvious curative effect on treating summer-damp cold. Due to the adoption of transdermal absorption, the patient does not to take the cream orally, and the cream is especially suitable for infants. Due to the adoption of unique mode of the externally applied cream, the drug can be easily spread on the skin, and the drug components can stay on the skin for a long time so that the skin can absorb the drug. The cream is also simple to use.
CN102786687A Polyasparaginyl-L-cysteine and polyasparaginyl-L-methionine with polymerization degree of 59, preparation method and application thereof The invention relates to a polymer with a structural formula of Ia or Ib, a preparation method and applications thereof, particularly relates to polyasparaginyl-L-cysteine and polyasparaginyl-L-methionine with a polymerization degree of 59, and also relates to a preparation method which comprises the following steps of dehydration condensation of DL-aspartate to generate polysuccimide with a polymerization degree of 59, and reaction with L-cysteine or L-methionine; the invention also provides nanometer structures of polyasparaginyl-L-cysteine and polyasparaginyl-L-methionine with a polymerization degree of 59, and applications of the polyasparaginyl-L-cysteine and polyasparaginyl-L-methionine as lead dispelling agents; the polyasparaginyl-L-cysteine and polyasparaginyl-L-methionine have the advantages of less toxic and side effect, suitability of oral administration, high selectivity, good transmembrane performance, and the like.
US20120077879 Process for making compositions with poorly compressible therapeutic compounds A process for preparing solid dosage forms that contain poorly compressible therapeutic compound. The process, for example, provides for the inventive use of an extruder, especially a twin screw extruder, to melt granulate a therapeutic compound(s) with a granulation excipient.
CN102186477A Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ("mGluR2") which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
US7211420 Oxidizing limonene or pinene or a cyclic sesquiterpene, wherein said limonene, pinene or cyclic sesquiterpene is optionally substituted by an alkyl of 1 to 6 carbons or an alkenyl of 1 to 6 carbons with a mutant haem-containing P450 enzyme, wherein mutant enzyme is a mutant of a P450BM-3 A process for oxidizing a substrate which is an acyclic or cyclic terpene, or a cycloalkene; or a substituted derivative thereof, which process comprises oxidizing said compound with a mutant haem-containing enzyme, the mutant comprising the substitution of an amino acid in the active site by an amino acid with a less polar side-chain. The enzyme is typically P450cam or P450BM-3. Cells and libraries of cells in which the process can be carried out or which can be used to select advantageous mutant enzymes are also provided.
EP1951708B1 Piperazine derivative useful as a ccr5 antagonist The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
CN102895459A Longevity-prolonging health-strengthening donkey-hide gelatin jelly The invention discloses a longevity-prolonging health-strengthening donkey-hide gelatin jelly which comprises milkvetch root, prepared rehmannia root, prepared fleeceflower root, donkey-hide gelatin, walnut kernel, black sesame, sliced dioscorea rhizome and yellow rice wine. The longevity-prolonging health-strengthening donkey-hide gelatin jelly tonifies qi, nourishes blood, is used for treating geromorphism, extremity weakness, soreness of loins and knees, amnesia and insomnia, can enhance immunity, anti-hypoxia capability and emergency response capability, removes free radicals, has a clear and definite effect, overcomes the existing problem of unclear differentiation of administration objects and functions of a health-strengthening jelly on the market and enables efficacy of the health-strengthening jelly to be maximally performed.
US20090286770 Use of Staurosporine Derivatives for the Treatment of Multiple Myeloma The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving ras or FGFR3 signalling pathways and l or c-fos transcription, especially for the curative and/or prophylactic treatment of myeloma or multiple Myeloma, and to a method of treating diseases involving ras or FGFR3 signalling pathways and/or c-fos transcription.
CN103393734A Beriberi liquor The invention discloses beriberi liquor, which is prepared by the following raw materials by weight: 5-10 parts of realgar, 1-5 parts of aloe, 20-30 parts of common cnidium fruit, 10-15 parts of rice vinegar, 5-10 parts of garlic, and 30-50 parts of alcohol. Realgar, common cnidium fruit and garlic are chopped and uniformly mixed, and then are immersed for about 10-20h in rice vinegar and alcohol.
WO2013163402A1 Methods for treatment of 16p11.2 microdeletion syndrome Subjects that have a 16p11.2 microdeletion syndrome are treated by administering compositions that include mGluR inhibitors, including mGluR antagonists that include mGluR negative allosteric modulators. Administration of compositions employed in the methods of the invention can treat psychiatric, including neuropsychiatric disorders, cognitive impairments, attention, obesity, intellectual disability and seizure disorders.
CN101062029A Application of wogonin in the preparing of medicine for treating gastric cancer The invention discloses an application of wogonin to prepare stomach cancer medicine in pharmacy domain, which is characterized by the following: possessing distinctive growth inhibitory action of the wogonin for human stomach cancer MGC803 bare mouse transplanting tumor. This invention provides better choice for stomach cancer patient.
US20120108569 8-AZA Tetracycline Compounds The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
US20110104065 Genetic alteration associated with pre-malignant cancer Described herein are progenitor cancer cells and cell lines isolated from human breast ductal carcinoma in situ (DCIS) lesions and the uses of these cells or cell lines in drug design, drug screening, and monitoring in vivo therapy. The DCIS malignant precursor cells or cell lines are epithelial in origin, are positive for markers of autophagy, show at least one genetic difference from normal cells of said fragment, form 3-D tube-like structures or ball aggregates, or are inhibited in formation of 3-D structures and migration by treatment with chloroquine. In one embodiment, there is a loss of heterozygosity (LOH) that is narrowly confined to a region of chromosome 6p (6p21.1-6p12.3) that contains the SUPT3H gene.
US20110082198 Theaflavin compositions, production, and methods to control physiological disorders in mammals A process for producing a purified extract comprising between about 40% and about 90% theaflavins is provided. Purified theaflavin extract produced by the disclosed process is provided which comprises less than about 5% TF1, between about 10% and about 60% TF2a, between about 5% and about 35% TF2b, and between about 10% and about 65% TF3. Individual dosage compositions are provided for the control of a physiological disorder comprising about 5% to about 95% theaflavins in a pharmaceutically acceptable vehicle or a dietary supplement vehicle. Further individual dosage compositions are provided which comprise an effective amount of substantially only one theaflavin species selected from the group consisting of TF1, TF2a, TF2b, and TF3. Individual dosage compositions are provided which comprise an effective amount of substantially only two theaflavin species selected from the group consisting of TF1 and TF2a, TF1 and TF2b, TF1 and TF3, TF2a and TF2b, TF2a and TF3, TF2b and TF3. Methods of treatment of human physiological disorders are provided which comprise administering oral dosage forms of the compositions.
US20120053148 Inhibitors of hepatitis c virus The present application includes novel inhibitors of HCV, compositions containing such compounds, therapeutic methods that include the administration of such compounds.
CN103222979A Grape anthocyanin component and pharmacological activity study The invention discloses an anthpcyanin component obtained from a grape, or grape skins or a mixture of the grape skins and grape seeds. A quality standard of the component is set, and a pharmacological study is carried out. The pharmacological study shows that the component has the pharmacological functions of being lipid-lowering and anti-oxidant, adjusting the secretion function of vascular endothelial cells and curing atherosis.
CN103687843A Quinone based nitric oxide donating compounds The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment of pathological conditions where a deficit of NO plays an important role in their pathogenesis.
EP1487821B1 Benzodiazepine-substituted piperidines for utilization in the treatment of cardiovascular diseases The invention relates to substituted piperidines of general formula (I), wherein R, R2 to R5, A, X, Z and n have the meaning defined in claim 1, to their tautomers, their diastereomers, their enantiomers, their mixtures and salts, especially their physiologically acceptable salts with inorganic or organic acids or bases. Said piperidines have valuable pharmacological properties, particularly CGRP-antagonistic properties. The invention also relates to medicaments containing said compounds, to the use thereof and to a method for the production of said compounds.
US7317016 Methods of treating medical conditions using sulfonate-substituted pyrazolopyridine derivatives This invention relates to methods of treatment of cardiovascular disorders, thromboembolic disorders, inflammation, and disorders of the central nervous system using pyrazol pyridine derivatives of formula (I) wherein R1 is a radical of the formula —O—SO2—R3 in which R3 is optionally substituted C1-6-alkyl, optionally substituted C3-8-cycloalkyl, or optionally substituted phenyl; R2 is H, optionally substituted C1-6-alkyl-CO— or optionally substituted C1-6-alkyl-SO2—; as well as salts, stereoisomers, tautomers, and hydrates thereof.
CN101570917B Method for preparing bio-adhesive medicament-carrying nano-fiber membrane by electro-spinning The invention relates to a method for preparing a bio-adhesive medicament-carrying nano-fiber membrane by electro-spinning, which comprises the following steps: (1) dissolving a polymer with bio-adhesive property and an artificially synthesized polymer in dimethylformamide according to the mass ratio of 0-10:0-10, continuously stirring and swelling the mixture for 24 hours at a temperature of between 55 and 60 DEG C, then cooling the mixture to normal temperature, and performing ultrasonic degassing for 12 to 20 minutes; and (2) adopting a flattened pinhead as a capillary for jetting trickles,connecting the capillary with a high-pressure generator, controlling the spinning liquid flow rate by a micro syringe pump, and receiving fibers by a grounded aluminum foil. The method is simple andhas low cost, and the prepared medicament-carrying nano-fiber membrane can be applied to simply preparing a functional membrane product which has functions of a transdermal medicament delivery system,a local medicament delivery system, nutrition and health care, convenient daily hygiene and the like.
CN102070531A Microwave radiation injury protection medicines The invention discloses microwave radiation injury protection medicines shown in a structural general formula (I). Molecules of the medicines contain nitronyl nitroxide radical structural units, the medicines have the characteristic of removing harmful free radicals in an organism subjected to microwave radiation injury, and have obvious effect of preventing and treating the microwave radiation injury.
CN102382129A Spirocycles-substituted phosphodiesterase inhibitor The invention belongs to the medicine technical field, more specifically relates to a spirocycles-substituted phosphodiesterase inhibitor or its pharmaceutically acceptable salt shown in a general formula (I), wherein R1, R2, R3, R4 and W are defined in an instruction. The invention also relates to a preparation method of the compound, a pharmaceutical composition and a preparation which contain the compound, and an application of the compound in preparation of medicines for treating and/or preventing sexual dysfunction diseases and other diseases caused by cGMP signal transduction disfunction.
US20050154230 Urea derivatives This invention relates to urea derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The urea derivatives of the present invention has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.
WO2009140275A1 Analogs of propofol, preparation thereof and use as anesthetics Compounds of formula (I) wherein X is H or F and pharmaceutically acceptable salts thereof are useful as anesthetics.
CA2574898C Immune modulation and anti-allergy activities of zingiber zerumbet The present invention provides for a method of preparing a nutraceutical formulation comprising the step of solvent extraction from the root of Zingiber zerumbet Sm, and the use of this formulation to regulate the immune system, and more specifically to prevent or to treat an allergic disorder.
US20080292713 Respirable Powders A spray dried dispersible powdered composition suitable for inhalation by a human subject, which composition comprises: a) at least one active agent suitable for treating a condition in said subject by inhalation; b) a hydrophobic amino acid; and c) a pharmaceutically acceptable biodegradable polymer.
EP2205596A1 (3-hydroxy-4-amino-butan-2-yl) -3- (2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease. (Formula)
WO2009111442A1 AMINO-QUINOXALINE AND AMINO-QUINOLINE COMPOUNDS FOR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS Compounds of the Formula (I), where W represents CH or N; and Q represents -CN, -C(=NOH)NH2, -CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
US6864068 Mutant plant Antifungal proteins which are analogues of the Rs-AFP2 protein and contain particular mutations in their amino acid sequence. The mutated proteins possess enhanced salt-tolerant antifungal activity. The proteins are useful for combating fungal diseases in agricultural, pharmaceutical or preservative applications.
CN1732955B Pharmaceutical composition making anemarrhena total sapogenin as active ingredient, its preparation method and use The invention provides a pharmaceutical composition using timosaponins as the active constituent, the process for preparing the pharmaceutical composition using timosaponins as the active constituent, and its use in preparing medicaments for treating or preventing climacteric metancholia, osteoporosis and vascular dementia.
CN101011529A Pharynx-clearing and throat-health-care medicament and its preparation The invention discloses a medicament for clearing pharynx and process for preparation, wherein the medicament comprises the following raw materials (by weight portion): emblic leafflower fruit 150-600 parts, honeysuckle flower 125-500 parts, arctium fruit 75-300 parts, ophiopogon root 50-200 parts, mentha-camphor 10-20 parts, vitamin C 30-120 parts, granulated sugar 315-1260 parts and glucose 135-540 parts.
US20110312875 Peptidic compounds The present invention provides a compound of formula I, II, III and IV as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention.
WO2011112889A2 β-MANNOSYLCERAMIDE AND STIMULATION OF NKT CELL ANTI-TUMOR IMMUNITY β-mannosylceramides or salts or solvates thereof in a pharmaceutically acceptable carrier, for use as a Type I NKT cell agonist in conjunction with a therapeutically effective amount of α-galactosylceramide or a salt or a solvate thereof, and/or at least one or more T-cell co-stimulatory molecules, disclosed. Compositions comprising β-mannosylceramide, as well as methods of treatment of tumors are also provided.
CN1891261A Ointment for treating burn and empyrosis, and its preparing method The present invention relates to a Chinese ointment preparation for effectively curing burn and scald. Said Chinese ointment preparation is made up by using hornet's nest, hanshuishi, mabaoyi, vermilion, bushy knotweed root, cockroach and sesame oil as raw material through a certain preparation process.
WO2010045017A1 Amines and sulfoxides of thieno [2,3-d] pyrimidine and their use as adenosine a2a receptor antagonists This invention relates to a novel thieno[2,3-d]pyrimidine, (A), and its therapeutic and prophylactic uses, wherein R1 and R2 are definedin the specification. Disorders treated and/or prevented include Parkinson's Disease.
EP1296951B1 5-chloro-3-(4-methanesulfonylphenyl)-6'-methyl- [2,3'] bipyridinyl in pure crystalline form and process for synthesis This invention encompasses the Form V polymorph of Compound A of structural formula (A) which is useful in the treatment of cyclooxygenase-2 mediated diseases. The invention encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising the Form V polymorph of Compound A. The invention also encompasses a process for synthesizing the Form V polymorph of Compound A.
WO2008135169A1 Nucleic acid-containing cosmetic and/or pharmaceutical preparations for treating epithelial tissue The present invention relates to nucleic acid-containing cosmetic and/or pharmaceutical preparations for treating epithelial tissue, and to the use of nucleic acids as chemosensitizers for treating hyperplasia of epithelial tissue, for improving skin appearance, for epilating or inducing hair loss.
US20090258944 Method for the manufacture of therapeutic compounds and compositions, compounds and compositions produced therewith, and their use Organic nitrites can be produced from a compound which is a mono/polyhydric alcohol or an aldehyde- or ketone-derivate thereof after de-aeration of the same, using NO gas, and stored in an environment saturated with gaseous NO. Organic nitrites produced according to the invention exhibit less impurities and improved storage stability compared to conventionally produced nitrites. The organic nitrites of the invention can easily be formulated into pharmaceutical compositions and have utility for the treatment of various conditions.
WO2014084298A1 Lsd1-selective inhibitor having lysine structure The present invention mainly addresses the problem of providing a novel compound having a LSD1-selective inhibitory activity and also having an anti—tumor/anti-cancer activity, an anti-virus activity and the like. As a means for solving the problem, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof is provided. [In the formula, R1 to R5, A, and *1 to *3 are as defined in the description.]
EP1816121A1 9-Chloro-15-deoxyprostaglandin derivatives, process for their preparation and their use as medicaments The present invention relates to 9-chloroprostaglandin derivatives of the general formula I which may be advantageous for the treatment of fertility problems.
US20110263687 Rna molecules and uses thereof The present invention relates to substantially single-stranded isolated RNA molecules comprising 18 to 19 contiguous nucleotides that corresponds to a non-protein-coding genomic DNA sequence located between −60 and +120 nucleotides from a transcription start site in a mammalian genome. Specifically, the isolated RNA molecules have a high GC content (>60%), are nuclear specific, and may be associated with aberrant gene regulation and/or transcription in various mammalian diseases and conditions. The isolated RNA molecules, modified RNA molecules and fragments thereof may be particularly useful for the diagnosis, prognosis and treatment of diseases such as Crohn's disease, Alzheimer's disease, Parkinson's disease, rheumatoid arthritis, myocardial infarction, diabetes, congenital developmental disorders, coronary heart disease and cancer such as breast cancer, lymphoma, leukemia, aggressive metastatic brain cancers, colorectal cancer, gastric cancer, ovarian cancer and pituitary tumors.
CN101049311A Compound Almitrine drop pills, and preparation technique A dripping pill of compound almitrine for treating subacute or chronic cerebrovascular insufficiency, cerebral apoplexy sequelae, senile dementia, dysmnesia, and ischemic cochleovestibular dysfunction is prepared from the almitrine bismesylate, raubasine and the matrix of dripping pill. Its preparing process is also disclosed.
CN103476770A Novel salts and polymorphic forms of afatinib Afatinib salts and crystalline forms thereof are described in the present application and processes for their preparation. Crystalline forms of Afatinib are also described in the present application and processes for their preparation. The present invention also includes pharmaceutical compositions of such Afatinib salts and crystalline forms thereof or crystalline forms of Afatinib, methods of their preparation and the use thereof in the treatment of a patient in need thereof.
US7871994 at least one ingestion period preceding the permanent administration of hormone daily units has an ingestion pause in which either no daily units or units with a much lower hormone content is given Method for hormone replacement therapy, in which at least in the established postmenopause a daily unit with at least one hormonal component, namely with at least estrogen (E) and/or at least one gestagen (G) is administered permanently and continuously every day, characterized in that in at least one ingestion period preceding the permanent administration of hormone daily units is provided an ingestion pause (P), in which either no daily units or placebos or daily units with a much lower estrogen and/or gestagen content than during the permanent administration of hormone daily units in the established postmenopause and during the ingestion phase(s) of the preceding ingestion period are administered, as well as administration form for hormone therapy.
EP2038267A2 Thiadiazolidinone inhibitors of ptpase Compounds of the formula (I) are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
WO2008092887A1 I-oxa-3-azaspiro (4.5) decan-2-one and 1-oxa-3, 8-diazaspiro (4.5) decan-2-one derivatives for the treatment of eating disorders The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, formula (I) wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1 -C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; W is -CZ1 or nitrogen; Z1 is hydrogen, C1 -C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; B is hydrogen or a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is -CZ1, compounds of formula (I) have a trans stereochemistry; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
CN103285082A Medicament composition for treating gynecological inflammation The invention relates to a medicament composition for treating gynecological inflammation. The medicament composition is prepared from raw materials including taxus chinensis active extracts, camphor and peppermint oil, and a pharmaceutical carrier as a substrate. The medicament composition provided by the invention can improve the comprehensive utilization value of taxus chinensis, and meanwhile, the prepared medicament composition has a better anti-inflammation effect.
US20080095853 Modified Release For Proton Pump Inhibitors An oral solid pharmaceutical dosage form comprising an acid sensitive proton pump inhibitor (PPI) as single active drug, releasing the PPI in two separate pulses, one immediate and one delayed. The PPI is formulated into a core material in the form of pellets, which are coated i.a. with a combination of a delayed release modifying layer and a lag time controlling layer. The pellets are further provided with an enteric coating layer. The application also relates to processes for preparing the dosage forms as well as their use in the treatment of gastrointestinal diseases.
US7579375 (2R,7R)-7-Hydroxy-2-propyloctanoic acid, (2R,7S)-7-hydroxy-2-propyloctanoic acid and (2R)-8-hydroxy-2-propyloctanoic acid; treating agent for neurodegenerative diseases such as brain infarction and Alzheimer's disease The present invention relates to a compound represented by formula (I) wherein R1 represents optionally protected hydroxy or oxo, indicates α-configuration, β-configuration or a mixture of these in an arbitrary proportion, n represents an integer of 1 to 3, and m represents 0 or an integer of 1 to 10; and wherein two or more R1's are not bound to the same carbon atom other than the terminal carbon atom, a salt thereof or a prodrug thereof. The compounds represented by formula (I) have an ability to improve astrocyte function, and they are useful as a preventive and/or therapeutic agent for a brain infarction, neuronal dysfunction by brain infarction, Parkinson's disease, Parkinson's syndrome, amyotrophic lateral sclerosis or Alzheimer's disease.
US20130005720 Pharmaceutical composition for treating cancer and applications thereof This invention relates to a pharmaceutical composition for treating cancer, comprising an effective amount of a compound represented by formula (I): wherein R is —CCOCCOCC— or —CCOCCOCCOCC—; and a pharmaceutical acceptable carrier. This invention also relates to a method for treating cancer, comprising administering a therapeutically effective amount of said compound to a subject; and a method for stabilizing G4 structure of telomere by using this compound.
US20120329831 Pharmaceutical composition of donepezil The present invention relates to a pharmaceutical composition of donepezil or pharmaceutically acceptable salts thereof comprising ethyl cellulose and methacrylic acid copolymer in a ratio of more than 1.3. Further, it relates to process for preparation of said composition.
WO2008137126A2 Combination therapy for the treatment of hcv infection The present invention relates to therapeutic combinations comprising a protease inhibitor and a polymerase inhibitor for the treatment of HCV. The present invention also relates to therapeutic combinations comprising VX-950 and a polymerase inhibitor. Also within the scope of the invention are methods using the therapeutic combinations of the present invention for treating HCV infection or alleviating one or more symptoms thereof in a patient. The present invention also provides kits comprising the combinations of the present invention.
CN102058582A Application of indole-2,3-diketone to preparing medicament for resisting aphronesia The invention relates to application of indole-2,3-diketone to preparing a medicament for resisting aphronesia. The indole-2,3-diketone is a natural product or an artificial synthesis product, has low toxicity, small side effect and the favorable functions of resisting the aphronesia and improving the learning and memory capabilities.
US7595342 Water-soluble strontium salts for use in treatment of cartilage and/or bone conditions Compounds and pharmaceutical compositions for use in the treatment and/or prophylaxis of cartilage and/or bone conditions and for methods of treating such condition. The compounds are salts of strontium that have a water-solubility of from about 1 g/l to about 100 g/l at room temperature, especially amino acid salts of strontium or dicarboxylic acid salts of strontium. Examples of novel water-soluble strontium salts are e.g. strontium glutamate and strontium alpha-ketoglutarate. The present invention also relates to an improved method for preparing the strontium salt of glutamic acid.
CN103739564A Multiple crystal forms of valsartan and preparation method thereof The invention belongs to the technical field of pharmaceutical chemistry, and discloses two new crystal forms namely a crystal form E and a crystal form F of valsartan and a preparation method thereof. The means of XRD (X-ray diffraction), microscopes Raman spectrometer, infrared spectrum, DSC (differential scanning calorimetry), TGA (thermal gravity analysis), DVS (dynamic vapor sorption) and the like are applied to perform comprehensive characterization on the new crystal forms and the fact that the new crystal forms have more excellent physical, chemical patent medicine properties is discovered. The preparation method of the new crystal forms of valsartan, disclosed by the invention, is simple, easy to control and good in reproducibility, and can be used for obtaining a target crystal form stably.
US20090155380 Non-medicinal food additive for animals, supplemented foods containing same and method for improving animal growth This invention relates to a non-medicinal food additive that is an animal growth promoter containing 99% pure zeolite partially or totally exchanged with a Cm+ cation, i.e., a synthetic zeolite, having the general formula I below: 1 m yC m + ( 1 - y ) 1 n M n + AlO 2 xSiO 2 in which x is greater than 1 and advantageously between 1 and 15; Mn+ represents an alkaline or alkaline earth exchangeable ion, advantageously Na+, K+, Ca2+ or Li+; n is between 1 and 2; y is the exchange rate and is between 0.001 and 1; Cm+ is a metallic cation chosen from among copper Cu2+, silver Ag+ or zinc Zn2+; m is between 1 and 2; this invention also relates to an additive premix and a supplemented food containing same and a method of improving the growth of animals.
US20090099264 Fluoroalkylamine Derivatives as Cathepsin Inhibtors The present invention provides compounds of formula I which are inhibitors of cathepsin S and as such are useful in the prevention and treatment of cathepsin S dependent diseases and conditions including, but not limited to, chronic obstructive pulmonary disease (COPD) and pain.
CN1839822A Injectable stable pharmaceutical composition containing active ingredient silibinin and its salt The invention relates to a pharmaceutical composition containing silybin or its salts as the active constituents, the composition also comprises water-soluble bulking agent, pH regulator, stabilizer, water for injection, and osmoregulation agent. The pH of the disclosed freeze-dried powder injection, injection and transfusion is between 7-9 under aqueous solution state, the stabilizing agent is preferably tris(hydroxymethylamino)methane. The pharmaceutical composition can be used for treating acute hepatitis.
WO2012011673A2 Pharmaceutical composition including hesperetin as an active ingredient for promoting muscle cell differentiation or renewal The present invention relates to a promoter of muscle cell differentiation or renewal, to a pharmaceutical composition for treating or preventing muscular impairment, and to a food composition for alleviating or preventing muscular impairment. The promoter of the present invention is effective for muscle cell differentiation and renewal, and the composition of the present invention is effective for the treatment (improvement) or prevention of muscular impairment.
WO2014054965A1 Combination for the prophylaxis and treatment of behavioural, mental and cognitive disorders The invention relates to the field of pharmacology and practical medicine, and specifically to the combined use of medicinal preparations, with neuro-tropic action, alleviating the manifestation of mental, behavioural and cognitive disorders in the event of organic damage of varying origin to the central nervous system. The combination comprises memantine and melatonin in therapeutically effective quantities. The combination makes it possible significantly to increase the effectiveness of treating diseases.
WO2006038112A1 Use of kinase inhibitors to promote neochondrogenesis This invention provides methods for utilizing compounds that inhibit cyclindependent kinase and tyrosine kinase enzymes in the promotion of neochondrogenesis and the enhancement, protection and repair of cartilage. In certain embodiments the invention relates to methods of using compounds of formula (I): and pharmaceutically acceptable salts thereof, to promote neochondrogenesis, wherein, R1,R2, R3, R4, R5, R6, A, B, D, and E have any of the values defined therefor in the specification.
WO2009143662A1 Pharmaceutical composition comprising calcium blocker and b family vitamins and the use thereof Pharmaceutical composition containing calcium channel blocker and B family vitamins and the use of the composition in treating hyperhomocysteinemia are provided. The combination of calcium channel blocker and B family vitamins can act on multiple paths and links of hyperhomocysteinemia, decrease organ damage effectively and reduce levels of homocysteine. It improves upon a single drug, and reavels the significant synergetic effect of calcium channel blocker and B family vitamins on the reduction of elevated levels of homocysteine and relief of the damage caused by elevated levels of homocysteine.
CN102198120A Medicinal use of lithospermi naphthoquinone compounds The invention discloses the use of lithospermi naphthoquinone compounds in the preparation of phosphodiesterase 4 inhibitor. The invention also discloses the use of the lithospermi naphthoquinone compounds in the preparation of medicines for treating asthma and chronic obstructive pulmonary diseases, the use in the preparation of medicines for treating inflammatory bowel diseases, the use in the preparation of medicines for treating rheumatoid arthritis, particularly the use in the preparation of medicines for treating ulcerative colitis and Crohn disease. The invention also discloses the medicinal use of one or several of lithospermi extracts.
EP2258347A2 Tamper-resistant products for opioid delivery Disclosed in certain embodiments is a dosage form comprising a plurality of extruded particles comprising an adverse agent or antagonist and a layer disposed about the particles.
US20090069340 Pyrazolone Compounds As Metabotropic Glutamate Receptor Agonists For The Treatment Of Neurological And Psychiatric Disorders Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, X, and n are as defined for Formula (I) in the description, processes for the preparation of the compounds and new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and the use of the compounds in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction.
CN103611154A Lophius litulon skin collagen peptide composition capable of resisting gram negative bacteria The invention discloses a lophius litulon skin collagen peptide composition capable of resisting gram negative bacteria. The lophius litulon skin collagen peptide composition is a compound solution formed by compounding a lophius litulon skin collagen peptide solution with the concentration of 100-200mg/mL and a florfenicol solution with the concentration of 20mu g/mL according to the volume rate of (3-4):1. According to the invention, lophius litulon skin collagen peptides and florfenicol are combined to synergically take effects, so that the resisting and inhibiting effects for the gram negative bacteria are better, meanwhile, the aims of reducing the dosage of antibiotics and the residues of drugs and avoiding or reducing the generation of drug-resistant strains are achieved, and the economic additional value of lophius litulon skin is increased.
WO2005123082A1 An anti-hyperlipemia composition The present invention offers an anti-hyperlipemia composition, containing Acipimox and Rosuvastatin, or their salts, esters and solvates. The proportion by weight is (15-100):1, preferably (40-100):1, more preferably 60:1. Acipimox can be used in combination with Rosuvastatin in synergistic action, the effect of anti-hyperlipemia is better than the combination of Acipimox and Lovastatin.
CA2387958C Method of preparing valproic acid compounds The invention relates to a method for producing compounds which contain at least one molecule valproinic acid salt and at least one molecule valproinic acid. The valproinic acid salt represents alkali or alkaline earth salt. Valproinic acid is directly converted with the calculated amount of the corresponding alkali carbonate or earth alkaline carbonate and/or the calculated amount of the corresponding alkali bicarbonate or earth alkaline bicarbonate without adding a solvent and at a temperature that is higher than the melting temperature of valproinic acid.
WO2010006125A3 2-methylene-19,26-dinor-(20r,22e,25r)-vitamin d analogs This invention discloses 2-methylene-19,26-dinor-(20R,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20R,22E,25R)-1α,25- dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti -cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows very low activity in vivo on bone calcium mobilization and relatively high intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
US20090263498 Pharmaceutical preparations for treating inflammatory diseases The present invention refers to a pharmaceutical preparation for treating inflammatory diseases and microbial infections comprising a pharmaceutically effective amount of ozone and at least one monomeric amino acid having an oxidation-sensitive side chain, or at least one ozonized monomeric amino acid having an oxidation-sensitive side chain. Also described is the use of a preparation as described before for providing a medicament for treating inflammatory diseases, microbial infections and for immune modulation. The pharmaceutical preparation according to the invention is particularly useful in the treatment of oral inflammations.
CN103505449A Application of N-acetylcysteine in preparation of drugs for preventing and treating DNA damage and tissue damage induced by synchrotron radiation The invention relates to an application of an antioxidant drug in the pharmaceutical science field, and especially relates to an application of N-acetylcysteine in preparation of drugs for preventing and treating gonads and other tissue DNA damage and tissue damage induced by synchrotron radiation X-rays. According to experimental results, N-acetylcysteine is indicated to be capable of protecting the double-strand DNA damage caused by synchrotron radiation X-ray radiation, and protecting testicular seminiferous tubule cell layer number reduction caused by the synchrotron radiation X-ray radiation; and the antioxidant is indicated to have important application value in the preparation of the drugs for preventing and treating the synchrotron radiation damage.
CN103450236A 6-Hydroxyloxoisoaporphine rare earth complexes, and synthetic method and application thereof The invention discloses a series of new 6-hydroxyloxoisoaporphine rare earth complexes, having a structural general formula as shown in specification, wherein Ln is La, Ce, Pr, Nd, Sm, Eu, Gd, Tb or Dy. The complexes are synthesized from 6-hydroxyloxoisoaporphine and the rare earth metal nitrates (Ln(NO3)3.xH2O as raw materials through a heating or reflux reaction. According to the complexes and the synthetic method and application thereof disclosed by the invention, the proliferation inhibition activity of the complexes to a plurality of human tumor cell strains such as SK-OV-3, SK-OV-3/DDP and T-24 is investigated, and results indicate that all of the complexes have remarkable antitumor activity in vitro; in particular, the 6-hydroxyloxoisoaporphine lanthanum complex has extremely remarkable activity to cervical cancer cells SK-OV-3; in addition, apart from the 6-hydroxyloxoisoaporphine europium complex, the other complexes all have a good inhibition effect on human ovarian cancer/cis-platinum persisters SK-OV-3/DDP.
US7897161 External medicine for treating dermatitis An external medicine for treating dermatitis wherein an adrenocortical steroid is included by a cyclodextrin; and 0.025 to 0.5% by weight of the adrenocortical steroid, 0.2 to 30% by weight of the cyclodextrin, and 0.5 to 55% by weight of dextran or pullulan are dissolved in an aqueous solution containing polysaccharide; and 0.5 to 55% by weight of xyloglucan, trehalose, laminaran, krestin, and pectin are blended. Grape sugar, mutan, lentinan, sodium chloride, and potassium chloride are comprised in the medicine. The medicine has a higher cure effect on atopic dermatitis and psoriasis vulgaris.
US20110166112 Method for stimulating platelet production Provided are methods for increasing platelet response in a subject at risk for bleeding due at least in part to a low platelet count by administering to a subject with a low platelet count an effective amount of 1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl]carbamoyl}pyridine-2-yl)piperidine-4-carboxylic acid.
US20070270382 Composition for Protecting Skin Disclosed are a composition for protecting skin and uses thereof. The composition comprises sphingomyelin as an active ingredient and protects the skin by inhibiting skin aging, treating a skin wound and improving a skin barrier.
EP2168951A1 Azolylmethylenehydrazine derivative and use thereof An azolylmethylidenehydrazine derivative represented by the formula (I) wherein Ar is an aryl group optionally having substituent(s), a heteroaryl group optionally having substituent(s) or a heteroaryl group optionally having substituent(s), R1 and R2 are the same or different and each is an alkyl group, a cycloalkyl group, an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), a heteroarylalkyl group optionally having substituent(s), or R1 and R2 are bonded to each other to form a nitrogen-containing heterocyclic group optionally having substituent(s), and X is CH or a nitrogen atom, or a pharmacologically acceptable salt thereof is useful as a medicament, particularly as an antifungal agent, or an anti-inflammatory agent or an antiallergic agent.
CN102670553A Venlafaxine hydrochloride osmotic pump controlled release tablet The invention provides a novel single-chamber tenlafaxine hydrochloride osmotic pump controlled release tablet preparation. A semi-permeable membrane containing ethyl cellulose (EC) and polyvidone (PVP) is coated on the surface of a medicament table core, so that the phenomenon of ageing of the semi-permeable membrane can be avoided, and medicament residues are reduced. The invention further provides a method for improving the anti-ageing performance of a single-chamber tenlafaxine hydrochloride osmotic pump controlled release tablet. The method is characterized in that: ethyl cellulose-polyvidone is taken as a semi-permeable membrane material. Moreover, the invention further provides an application of an ethyl cellulose-polyvidone composition to preparation of a single-chamber tenlafaxine hydrochloride osmotic pump controlled release tablet with anti-ageing performance.
US20080247992 N-Carboxyalkyl-1-cyclohexyl-2-substituted phenylbenzimidazole-5-carboxamides (2-[(1-cyclohexyl-2-{2-fluoro-4-[3-(aminocarbonyl)-6-(4-chlorophenyl)benzyloxy]-phenyl}-1H-benzimidazole-5-carbonyl)-amino]-3-(5-hydroxy-1H-indol-3-yl)-propionic acid); Flavivirus family infections such as hepatitus C Disclosed are compounds, compositions and methods for treating Flaviviridae family virus infections.
EP1651270B1 Medicaments for inhalation comprising betamimetics and an anticholinergic The present invention relates to novel pharmaceutical compositions based on beta2 agonists and salts of an anticholinergic, processes for preparing them and their use in the treatment of respiratory complaints.
US20120135085 Method and composition for disinfection and purification A method and composition for a non-toxic aqueous silicon solution.
US20100280070 Novel tetrahydroquinolines as aromatase inhibitors The invention relates to synthesis and biological screening of novel tetrahydroquinolines of formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them for aromatase inhibition: (I). The present invention also relates to a process for the preparation of the novel tetrahydroquinolines, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in for aromatase inhibition, particularly in the treatment and/or prevention of cancer, particularly breast cancer, more particularly hormone dependent breast cancer.
WO2009038112A1 Solid preparation comprising npyy5 receptor antagonist Disclosed is a preparation in which the solubility of an NPYY5 receptor antagonist in water can be improved even when the NPYY5 receptor antagonist is contained therein at a high content. Specifically disclosed is a solid preparation comprising an NPYY5 receptor antagonist, an amorphia-stabilizing agent, and optionally a crystalline-to-amorphous transformation-inducing agent. More specifically, the solid preparation contains hydroxypropylmethylcellulose phthalate and/or hydroxypropylmethylcellulose acetate succinate as the amorphia-stabilizing agent and urea and/or sodium saccharin as the crystalline-to-amorphous transformation-inducing agent in the total amount of less than 8 wt%. In the solid preparation, the elution of an NPYY5 receptor antagonist, which is poorly soluble in water, can be improved satisfactorily.
CN103356600A Application of Chukrasone B in anti-helicobacter pylori medicines In vitro activity experiments show that Chukrasone B has strong anti-helicobacter pylori (Helicobacter pylori, Hp) activity. The Chukrasone B can be used for treating diseases such as acute and chronic gastritis, gastric ulcer and duodenal ulcer and preparing medicines for treating diseases such as acute and chronic gastritis, gastric ulcer and duodenal ulcer. The use of the Chukrasone B in anti-helicobacter pylori medicines provided by the invention is disclosed for the first time. As the framework type belongs to a brand-new framework type, and the inhibitory activity of the Chukrasone B to helicobacter pylori is unimaginably strong, the probability of giving any enlightenment by other compounds does not exist. The Chukrasone B has remarkable substantial characteristics and meanwhile has a remarkable progress for preventing and treating helicobacter pylori infection.
CN103405384A Pharmaceutical composition of tranexamic acid The invention belongs to the technical field of medicines, discloses a pharmaceutical composition of tranexamic acid, and particularly relates to a pharmaceutical composition containing tranexamic acid and organic acid. The pharmaceutical composition can be prepared into injection; the high-temperature and high-light tests show that the impurities, namely, cycloolefin, aminomethylbenzoic acid and a Z-isomer, and the total impurities of the injection meet the quality requirements. A preparation prepared from the pharmaceutical composition has the advantages of high stability and low impurity content.
EP1705176A1 Carboxamide derivative and use thereof The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B and ring C are each an aromatic ring optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), Z is an optionally halogenated C1-6 alkyl group, Y is a methylene group optionally having substituent(s), m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and
CN102895268A Lipid-lowering composition The invention discloses a lipid-lowering composition prepared from, by weight, 5-15 parts of red monas rice, and 5-10 parts of curcumin. The lipid-lowering composition provided by the invention has a substantial weight-reducing and lipid-lowering effect, and low adverse reaction. The composition is safe and reliable, such that the composition can be developed into novel weight-reducing and lipid-lowering medicines or health-care foodstuffs.
WO2006125285B1 Insulin sensitization to slow down pubertal tempo and to augment pubertal growth In accordance with the purpose of the invention, as embodied and broadly described herein, the invention is broadly drawn to a new method of treatment, the use of agents to manufacture a composition of treatment or the composition of treatment for the prevention of rapidly progressive puberty, the prevention of early menarche or the modulation, more particularly the delay, of the tempo of puberty in a female mammal, preferably a human girl, and the disorders related thereto. In a particular embodiment the present invention involves the use of at least one insulin-sensitizing agent such as metformin, any of the polymorphs of metformin or a pharmaceutically acceptable salt thereof for the preparation of a composition of treatment to modulate the tempo of pubertal progression in a girl.
US7495018 An enzyme inhibitor of p38 MAP kinase, an antagonist of tumor necrosis factors or adenosine receptor, a thiazole with the 5-pyridyl group derivatives (1) A 1,3-thiazole compound of which the 5-position is substituted with a 4-pyridyl group having a substituent including no aromatic group or (2) a 1,3-thiazole compound of which the 5-position is substituted with a pyridyl group having at the position adjacent to a nitrogen atom of the pyridyl group a substituent including no aromatic group has an excellent p38 MAP kinase inhibitory activity.
CN103211771A Ramosetron hydrochloride freeze-dried powder injection and preparation method thereof The invention discloses a ramosetron hydrochloride freeze-dried powder injection and a preparation method thereof. Under illumination, the solution of the existing ramosetron hydrochloride has poor stability, poordrug effects and high drug adverse effects; and the solids of the existing ramosetron hydrochloride have good stability. Therefore, the ramosetron hydrochloride freeze-dried powder injection improves product stability and safety. A preclinical research shows that an antagonistic activity of ramosetron hydrochloride to 5-HT3 acceptors is stronger and more stable than that of the existing 5-HT3 acceptor antagonist; and ramosetron hydrochloride has stronger effect of treatment on chemotherapeutic drug-caused emesis. Therefore, ramosetron hydrochloride is clinically used for preventing and treating digestive tract symptoms such as nausea and emesis caused by cancer-resistant drugs.
CN101049312A Composition of medication, preparation method and application A composite medicine for treating various bacterial and viral infections is prepared from the Yanhuning (dehydroandrographolide0potassium sodium succinate), cephalo- type antibiotics, and medicinal auxiliaries. Its preparing process is also disclosed.
US6887883 Combating angiogenic activity in a human comprising administering to a chrysanthone compound A series of compounds of natural origin are described, as useful agents for the treatment of diseases characterised by abnormal angiogenesis. These compounds are: chrysanthone A having formula (I); chrysanthone B having formula (II); and chrysanthone C having formula (III).
US20080181852 water soluble polyglutamnylglutamine conjugated to drugs, polydentate ligands, targeting, optical imaging, magnetic resonance imaging or stabilizing agents, having improved bioavailability Various biodegradable polyglutamate-amino acids comprising recurring units of the general formulae (I) and (II) are prepared. Such polymers are useful for variety of drug, targeting, stabilizing and/or imaging agent delivery applications.
CN101352409A Diclofenac sodium in situ forming eye gel The invention discloses a diclofenac sodium eye ophthalmic gel and a preparation method thereof; every 1000ml of the diclofenac sodium eye ophthalmic gel contains 0.1-2g of diclofenac sodium, 0.05-1g of preservative, 1.0-7.5g of osmoregulation agent, 30-150g of gel stroma, and rest amount of acid-base buffering agent and water used for injection. Due to the optimization and technique improvement of the auxiliary materials, the medicine dosage forms of the chloramphenicol are enriched, detention time of the medicine in the eyes are greatly prolonged, the healing effect is improved, and no pessimal stimulation response exists.
US20100286191 2-Arylthiazole Derivatives as CXCR3 Receptor Modulators The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
WO2011007551A1 Sugar alcohol-containing antibacterial agent for inhibiting proliferation of periodontal disease-causing bacteria Disclosed is an antibacterial agent having ameliorating and prophylactic effect on periodontal diseases and dental caries, which is characterized by the inhibitory effect of a sugar alcohol on proliferation of periodontal disease-causing bacteria and dental caries-causing bacteria. Specifically disclosed is an antibacterial agent for inhibiting proliferation of periodontal disease-causing bacteria, which contains a sugar alcohol, in particular lactitol or maltitol, as an active ingredient.
WO2008091161A1 Cosmetic composition containing spermine and emu oil Composition in form of a cream, liniment or oil for application on the skin for treatment of skin conditions such as wrinkles, burns, sunburns, aging, tired and stressed skin, and distinguished by the inclusion of a mixture of spermine, emu oil and possibly aloe vera. The composition may additionally contain one or more of the additives chosen among the group of preservatives, buffers, pigments, fragrances, stabilizing agents, gel forming agents, preservatives, oils, antibiotic agents, vitamins, water, thickening and neutralising ingredients.
US20100029781 Methods for preparation of anti-acne formulation and compositions prepared thereby The present invention provides methods to make solvent-microparticle (SMP) topical formulations for bioactive drugs. The formulations, which are aqueous gels containing undissolved solid drug, include a drug in a solution which can permeate the stratum corneum layer of the epidermis and the drug in an undissolved microparticulate solid form that does not readily cross the stratum corneum. The solid form is retained in or above the stratum corneum to serve as a reservoir or to provide drug action in the supracorneum zone. The fine, particulate solid component of the invention can confer a smooth, nongritty feel against the skin.
CN101175732B Production method for quinazoline derivatives and its application for producing medicine used for treating tumor disease Provided are quinazoline derivatives of the compound (I), and its preparation process and application as a medicine of inhibit tumor growth. The group X, Y, Z, R1, R2, R3, R4 of compound (I) are defined in the description. Compounds of the invention can specially inhibit tyrosine kinase activity, inhibit the activity of two high-affinity receptors of VEGF, adjust VEGF secretion, thus to have to achieve the purpose of treating malignant tumor.
WO2013182905A3 Mechanism, diagnostic, and treatments for complications of renal failure Mechanisms for complications of renal failure and processes for treating the same are disclosed. They include contacting a biological fluid (e.g. blood) with a filter body, the filter body having immobilized thereon either a CD36 receptor or a CD36 receptor fragment or a SCARB1 receptor or a SCARB1 receptor fragment, the blood having a reduced quantity of oxidatively modified proteins after contacting the filter body. They also include administering an antagonist drug to a patient that blocks the binding activity of the RAGE receptor or the CD36 receptor or the SCARB1 receptor. Diagnostic methods are also provided.
US7135488 Pyrrolyl-thiazole derivatives The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.
WO2008121859A1 Methods of using tricyclic compounds in treating sodium channel-mediated diseases or conditions This invention is directed to compounds of formula (I): wherein,, n, r, q, R1, R2, R3 and R4 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, pharmaceutical compositions comprising the compounds and methods of using the compounds and the pharmaceutical compositions for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
US20120309705 Novel 3'-deoxy-3'-methylidene-beta-l-nucleosides The present invention includes novel 3′-deoxy-3′-methylidene-β-L-nucleosides, pharmaceutical composition comprising such compounds, as well as the methods to treat or to prevent viral infections and in particular HBV and/or HIV infections. In accordance with the present invention, there are provided compounds represented by Formula (I), wherein B is selected from A1 and A2;
CA2505569A1 Attenuation of disorders by aminoglycosides The present invention provides a method of attenuating side effects caused by aminoglycosides by administering aminoguanidine either before or during the treatment with the aminoglycoside. The invention also provides compositions and kits for use in the treatment of infections that use aminoglycosides that can cause side effects such as nephrotoxicity and ototoxicity.
US20070219177 Agent for treatment of cerebral ischemic diseases A pharmaceutical composition for the treatment and/or prevention of cerebral ischemic diseases, which comprises two components, i.e. an astrocyte function-improving agent, preferably a compound represented by the formula (I): (wherein R6 is hydroxy, etc., (1) n is 1, R11 is hydrogen and R5 is (alkyl of which one carbon atom is substituted by fluorine)-CH2— or (2) n is 0 or 1, R11 is hydrogen, etc., and R5 is alkyl, etc.) and a thrombolytic agent, preferably tissue plasminogen activator, as active ingredients. The pharmaceutical composition of the present invention exhibits a synergistic therapeutic effect compared to independent administration of an astrocyte function-improving agent and a thrombolytic agent.
EP1784188A2 Fused triazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DPP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
WO2013173417A3 Glucokinase activator compositions for the treatment of diabetes The present invention relates to pharmaceutical compositions comprising {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid (FRI-1) in combination with an anti-diabetic drug selected from the group consisting of metformin, sitagliptin or exenatide. The present invention also relates to the use of the pharmaceutical compositions in restoring insulin sensitivity and treating type II diabetes, including reducing body weight in subjects undergoing type II diabetes treatment.
CN101757051A External medicine for removing foot odor and preparation method thereof The invention discloses an external medicine for removing foot odor, of which the formula comprises the components of alum, borax, salicylic acid, boric acid, hexamethylene tetramine, aspirin, urotropine, shi xiang, realgar, sulfur and ferrous sulfate. The proportion of the prescription is shown as follows: 30 parts of alum, 30 parts of borax, 30 parts of salicylic acid, 30 parts of boric acid, 30 parts of hexamethylene tetramine, 30 parts of aspirin, 30 parts of urotropine, 30 parts of shi xiang, 30 parts of realgar, 30 parts of sulfur and 580 parts of ferrous sulfate. The preparation method comprises the following steps: firstly, the alum, the borax, the boric acid and the ferrous sulfate are mixed, fried and dehydrated and then mixed uniformly with the alum, the salicylic acid, the hexamethylene tetramine, the aspirin, the urotropine, the shi xiang, the realgar and the sulfur and grinded by a grinder and finally screened. The external medicine has long medical effect, good foot odor removing effect and radical treatment.
CN102670484A Mannose-modified solid lipid nanoparticle plural gel and preparation method thereof The invention discloses a preparation method of a mannose-modified solid lipid nanoparticle plural gel. The preparation method comprises the following steps: 1), dissolving astragaloside and solid lipid material into ethanol to form matrix solution, adding emulsifier water solution in the matrix solution and stirring evenly to form suspension containing solid lipid nanoparticles, and adding waterto suspend after centrifugation to form purified solid lipid nanoparticles; 2), Modifying mannose through a solvent evaporation method, a high pressure homogenization method or microemulsion method to obtain purified solid lipid nanoparticles; 3), adding gel matrix and water into the mannose-modified solid lipid nanoparticle to obtain the mannose-modified solid lipid nanoparticle plural gel. The invention further discloses a mannose-modified solid lipid nanoparticle plural gel which is convenient in administration, can increase the drug solubility and achieves the purposes of slowly releasingdrugs, prolonging the administration time, reducing the administration times and improving the bioavailability of the drugs.
CN101932318A Composition for stimulating natural killer cell activity The present invention relates to a nutritional composition comprising dietary fibre for stimulating natural killer cell activity, in particular in patients infected with HIV, oncology patients and elderly.
US7425356 Liquid crystalline polymers mixture:, display, optics, diagnosis The invention relates to chiral compounds of formula I wherein X1, X2, X1, X2, x1, x2, y1, y2, B, C, U1, U2, V1, V2, W1 and W2 have the meaning given in claim 1, to liquid crystal mixtures comprising at least one chiral compound of formula I, to chiral linear or crosslinked liquid crystal polymers obtainable by polymerizing a polymerizable mixture comprising at least one chiral compound of formula I, to the use of chiral compound of formula I and mixtures and polymers obtained thereof in liquid crystal displays, active and passive optical elements, adhesives, synthetic resins with anisotropic mechanical properties, cosmetic and pharmaceutical compositions, diagnostics, liquid crystal pigments, for decorative and security applications, nonlinear optics, optical information storage or as chiral dopants, and to a liquid crystal display comprising a mixture comprising at least one chiral compound of formula I.
US7385042 Structurally distinct radionuclide complexes of multinitrogen heterocycles having phosphonic acid groups that target bone, and thus, are useful as imaging and therapeutic agents (e.g., for bone marrow suppression, cancer, bone pain) One embodiment provides a composition comprising a) a compound of formula I: wherein R1, X and n have any of the values described in the specification, or a pharmaceutically acceptable salt thereof; b) a radionuclide; and c) a radioprotectant.
US7381424 Hydrostatic delivery system for controlled delivery of agent The present invention provides a hydrostatic delivery system comprising a hydrostatic couple and an agent of interest. The hydrostatic couple comprises, at least one hydrodynamic fluid-imbibing polymer, and at least one hydrostatic pressure modulating agent. This delivery system has the ability to control the release of one or more agent of interest within a fluid environment following zero-order kinetics.
WO2010109050A1 Cromenopyrazole derivatives as cannabinoid receptor ligands The invention relates to compounds derived from cromenopyrazoles that are cannabinoid receptor ligands, to the use thereof for the production of a drug, to the use of this drug in the treatment and/or prevention of disorders associated with cannabinoid receptors, to the use of said compound as a reagent in biological assays related to cannabinoid receptors, and to the method for obtaining same.
US20080234383 Novel Compounds, Isomer Thereof, or Pharmaceutically Acceptable Salts Thereof as Vanilloid Receptor Antagonist; and Pharmaceutical Compositions Containing the Same This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receotor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.
US20110008269 Compositions and Methods Which Modulate G-Protein Signaling for the Treatment of Inflammatory Disorders such as Asthma and Allergic Conjunctivitis Compositions and methods for the treatment of asthma and inflammatory ocular disorders are disclosed.
CN101633672B Novel nucleoside compound as well as preparation method and application thereof The invention discloses a novel nucleoside compound shown as the general formula (I) as well as a preparation method and an application thereof. The compound has antiviral activity and is used for preparing antiviral medicines.
WO2012035123A1 Arylosulfonamides for the treatment of cns diseases Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.
US20080094573 Surface-modified materials, such as contact lenses, methods and kits for their preparation, and uses thereof Modified contact lenses and surfaces, methods for their preparation, and corresponding kits are disclosed. Also disclosed are uses of the contact lenses, such as for the administration of an agent to the eye.
WO2007043853A1 Pharmaceutical compositions comprising combined antidiabetic substances for use in diabetes mellitus The invention relates to the pharmaceutical industry in general and, in particular, to the pharmaceutical industry involved in the preparation of medicaments for controlling diabetes. More specifically, the invention relates to a composition comprising a combination of different types of antidiabetic substances. The composition is characterised in that the aforementioned combination or association consists of two or three antidiabetic substances that are selected from the group containing: sulfonylureas, meglitinides, biguanides or inhibitors of alpha-glucoside with thiazolidinediones for the treatment of type 2 diabetes mellitus in novel formulations. The composition is also characterised in that the sulfonylureas are selected from the group containing glipizide, glyburide, glimepiride; meglitinides, repaglinide, nateglinide, thiazolidinediones or a combination of same; biguanides such as metformin; inhibitors of alpha-glucoside known as acarbose, miglitol associated or combined with thiazolidinediones known as pioglitazone, rosiglitazone, troglitazone, such as a base or a physiologically-accepted salt.
CN103694084A Preparation method and application of menthol water-soluble compound The invention discloses a preparation method and application of a menthol water-soluble compound, and belongs to the technical field of chemical engineering. The preparation method comprises the following steps: (1) adding sodium or potassium into a menthol ether or alcohol solution in a nitrogen atmosphere, slowly stirring for full reaction, and standing for the whole night; (2) filtering and concentrating a mixture obtained from the step (1), washing, drying and collecting solids; (3) dissolving the solids obtained from the step (2) in water, dialyzing by an osmotic membrane, and decompressing for water removal to obtain the menthol water-soluble sodium or potassium salt. According to the preparation method for preparing menthol into the menthol water-soluble sodium or potassium salt through the steps, the characteristic of water insolubility of menthol is changed, the obtained product can be very easily dissolved in water, and the convenience is brought to subsequent processing; in addition, the novel application of the menthol water-soluble sodium or potassium salt is developed.
CN101618025B Veterinary doxycycline hydrochloride freeze-dried preparation and preparation method thereof The invention discloses a veterinary doxycycline hydrochloride freeze-dried preparation and a preparation method thereof, the veterinary doxycycline hydrochloride freeze-dried preparation consists of an active component of doxycycline hydrochloride and medical excipients, the medical excipients comprise lysine, sodium sulfite and polyvinyl pyrrolidone, the weight ratio of doxycycline hydrochloride to lysine is 1:0.8-1:1, the weight ratio of doxycycline hydrochloride to sodium sulfite is 1:0.01-1:0.05 and the weight ratio of doxycycline hydrochloride to polyvinyl pyrrolidone is 1:0.05-1:0.1. The preparation method comprises the steps of adding lysine, sodium sulfite and polyvinyl pyrrolidone in doxycycline hydrochloride according to the weight ratio, placing solution after the filtration in a tube antibiotics glass vial after sub-packaging treatment, carrying out semi-tamponade and vacuum freeze-drying, thereby obtaining the veterinary doxycycline hydrochloride freeze-dried preparation. The preparation can lead the pH value to achieve 8-8.33 after re-dissolution, thereby thoroughly solving the problem of lower pH value of the doxycycline hydrochloride veterinary drug; and the prepration is non-toxic and has the advantages of easy transportation, long storage time, no degeneration, good stability, very small intramuscular injection stimulation, low manufacturing cost and the like.
US20110281939 Polynucleotide aptamer-based cross-linked materials and uses thereof In one aspect, the disclosure provides cross-linked materials that include multivalent polynucleotide aptamers that bind a target molecule; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, wherein the two or more affinity ligands compete with the target molecule for binding with the aptamers and wherein conjugates are cross-linked within the material as a result of non-covalent interactions between aptamers and affinity ligands on different conjugates. These materials are designed to release amounts of conjugate in response to desired concentrations of the target molecule. Depending on the end application, in various embodiments, the conjugates may also include a drug and/or a detectable label. The drug, detectable label and affinity ligands may be covalently or non-covalently bound to the conjugate framework.
US20080090862 Isoquinoline Derivatives as Calpain Inhibitors The invention relates to derivative compounds of partially-reduced isoquinoline with substitution of a sec-butyl group at position 3 with calpain inhibitor activity. The inventive compound comprises an ester or amide derived from (3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-yliden)-acetic acid and (3-sec-butyl-1-thioxo-2, 3-dihydro-1H-isoquinolin-4-yliden)-acetic acid. Compounds having formula I or II can be used in the preventive or therapeutic treatment of a degenerative disease.
CA2791914A1 Nuclear transport modulators and uses thereof The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
CN101095677A Application of sophocarpine and the medicine salt thereof in the preparing of the medicine for increasing interferon The invention discloses the sophocarpine or its medical salt application in preparing medicine that can increase interferon content. Said sophocarpine medical salt is bromate or hydrochlorate or fluorate of sophocarpine. Said medical dosage form is any form that is medical acceptable. The sophocarpine or its medical salt can induce the interferon generation, which is effective for antiviral action.
CN103508951A Salts of 2-hydroxy-1-methoxyaporphine derivative The invention relates to fumarates of 2-hydroxy-1-methoxyaporphine and 2-hydroxy-1-methoxyaporphine derivatives or pharmaceutically acceptable solvates thereof, and an application of the fumarates or the solvates in preparation of acetylcholinesterase inhibitor drugs.
US20080139453 Comprising an emulsifying crosslinked siloxane elastomer, a hydrophobically modified polymeric emulsifier, a solvent for the emulsifying crosslinked siloxane elastomer and water; for moisturizing, protecting and/or treating the skin and/or keratinous fibers; sunscreen The present invention relates to an O/W/O emulsion comprising; a) an external oil phase which comprises an emulsifying crosslinked siloxane elastomer and a solvent for the emulsifying crosslinked siloxane elastomer; and b) an O/W type primary emulsion which comprises an internal oil phase dispersed in an aqueous phase dispersed in the external oil phase wherein the aqueous phase comprises from about 0.01% to about 10% of a hydrophobically modified polymeric emulsifier, wherein when shear stress is applied to the O/W/O emulsion during spreading on skin, at least a portion of the primary emulsion is released from the O/W/O emulsion. The present invention also relates to an O/W/O emulsion composition comprising: a) from about 0.1% to about 15% of an emulsifying crosslinked siloxane elastomer; b) from about 0.01% to about 10% of a hydrophobically modified polymeric emulsifier; c) from about 1% to about 40% of a solvent for the emulsifying crosslinked siloxane elastomer; and d) water, wherein when shear stress is applied to the composition during spreading on skin, phase separation is occurred.
WO2012072713A3 Lysine demethylase inhibitors such as cyclylcyclopropanamine derivatives for use in the treatment of diseases and disorders associated with flaviviridae The invention relates to methods and compositions for the treatment or prevention of Flaviviridae infections. In particular, the invention relates to an LSD1 inhibitor such as 2 - cyclyldyclopropan - 1 - amine derivatives, phenelzine derivatives and propargylamine derivatives for use in treating or preventing Flaviviridae infections, including hepatitis C virus infections.
WO2007069933A1 Method for decreasing postprandial glucose excursion The invention relates to the method for decreasing postprandial glucose excursion in a mammal in need thereof comprising a step of administering to said mammal an effective amount of water comprising from 99.76 to 99.99 molecular % of isotopologue 1H2160 at 0 to 240 min from the start of ingestion of a meal. Preferably, the effective amount water comprising from 99.76 to 99.99 molecular % of isotopologue 1H2160 is administered orally. Preferably, the effective amount of the water comprising from about 99.76 to about 99.99 molecular % of isotopologue 1H2160 is 0.1 to 20 g/kg body weight of a mammal. Further, invention relates to the medical food for decreasing postprandial glucose excursion in a mammal in need thereof which comprises water comprising from about 99.76 to about 99.99 molecular % of isotopologue 1H2160. Further, invention relates to use of water comprising from about 99.76 to about 99.99 molecular % of isotopologue 1H2160 for the manufacture of a medical food for decreasing postprandial glucose excursion in a mammal in need thereof. Preferably, the mammal is human.
CN102786401A Phenylpolyene compounds and their preparation method and use The invention belongs to the fields of pharmacy, relates to phenylpolyene compounds and especially relates to (4E,8E)-1-(2,4-dihydroxyphenyl)-5,9,13-trimethyl-4,8,12-trialkenyl-1-one (1), (4E, 8E)-1-(2-hydroxy-4-methoxyphenyl)-5,9,13-trimethyl-4,8,12-trialkenyl-1-one (2) and (4E, 8E)-1-(2,4-dihydroxyphenyl)-2-hydroxy-5,9,13-trimethyl-4,8,12-trialkenyl-1-one (3) in Ferula spp., and their preparation method and use in inhibition of multdrug-resistant staphylococcus aureus. The (4E,8E)-1-(2,4-dihydroxyphenyl)-5,9,13-trimethyl-4,8,12-trialkenyl-1-one (1) has effects of inhibiting six types of drug-resistant staphylococcus aureus, and compared with control drugs of tetracycline and oxacillin, the (4E,8E)-1-(2,4-dihydroxyphenyl)-5,9,13-trimethyl-4,8,12-trialkenyl-1-one (1) has obviously stronger activity of inhibition of a drug-resistant staphylococcus aureus strain XU212 containing a TetK tetracycline efflux protein and a methicillin-resistant staphylococcus aureus EMRSA-16 strain containing a mecA gene protein. The (4E, 8E)-1-(2-hydroxy-4-methoxyphenyl)-5,9,13-trimethyl-4,8,12-trialkenyl-1-one (2) selectively has strong activity of inhibition of the drug-resistant staphylococcus aureus strain XU212 containing a TetK tetracycline efflux protein. The (4E, 8E)-1-(2,4-dihydroxyphenyl)-2-hydroxy-5,9,13-trimethyl-4,8,12-trialkenyl-1-one (3) has good effects of inhibiting six types of drug-resistant staphylococcus aureus. The phenylpolyene compounds provided by the invention can be used for preparation of multiple antibacterial injections, oral drugs and external drugs.
CN102908344A Pharmaceutical composition comprising meropenem, and preparation method and application therof The invention provides a pharmaceutical composition comprising meropenem, and a preparation method and application thereof. The pharmaceutical composition is composed of meropenem and anhydrous sodium carbonate. Production verification demonstrates that: the composition can overcome defects of conventional meropenem compositions, such as poor dissolvability and stability, poor fluidity during filling process, large loss, low qualification rate, and uncertain product quality. The production process is simple and has high industrialization degree. Anhydrous sodium carbonate as pharmaceutical adjuvant can improve dissolvability of meropenem, improve product stability, guarantee clinical administration safety, and improve product quality.
WO2005080319A1 Hydrazino alcohol derivatives useful as inhibitors of copper-containing amine oxidases The invention relates to hydrazino alcohol derivatives of Formula (I) wherein ; R1 is hydrogen, lower alkyl or an optionally substituted phenyl or heteroaryl group; R2 is hydrogen or lower alkyl, or R1 and R2 may form together with the nitrogen atom to which they are attached a saturated heterocyclic ring; R3 - R5 represent each independently hydrogen, lower alkyl, aralkyl, optionally substituted phenyl or a heteroaryl group, or R2 and R3 may form together with the atoms to which they are attached a saturated heterocyclic ring, or R3 and R5 may form together with the carbon atoms to which they are attached a saturated carbocyclic ring; R6 is naphtyl, phenyl, substituted phenyl or a heteroaryl group; R7 is hydrogen, lower alkyl or aralkyl; n is 1, 2 or 3; and X = O, S, SO, SO2 or NR2. The compounds of Formula (I) are useful as inhibitors of copper-containing amine oxidases.
CN1879635A Beta-cyclodextrin inclusion compound of adefovir dipivoxil and preparation thereof The invention discloses a beta-cyclodextrin inclusion complex of adefovir dipivoxil and its preparing process, wherein the complex has the advantages of higher stability, better water-solubility, and quicker dissolving out speed. The complex can be used for preparing hepatitis-treating medicinal compositions.
WO2009070829A1 Non-aqueous oil-based fentanyl compositions for transmucosal administration The invention provides a composition and method of treating pain using the composition, the composition comprising a solution of at least one active agent selected from the group consisting of fentanyl, a derivative of fentanyl and an analogue of fentanyl in at least one non-aqueous oil-based solvent for transmucosal administration.
US7259270 Supermolecular carboplatin derivatives, their preparation and pharmaceutical composition containing them as active ingredient and applications of the compositions The present invention relates to a novel class of supermolecular carboplatin derivatives represented by general formula (I), wherein B is a polycarboxylic acid represented by general formula (II), wherein R1, R2 and n are defined as in the description. The present invention also relates to a process for preparing the same, pharmaceutical compositions containing the same as active ingredient and the use of the derivatives in the preparation of pharmaceutical compositions which are useful in treating various cellular cancers including hepatoma, stomach cancer, lung cancer and the like. The derivatives have stable cage-like chemical structures and constitutions in solid and in aqueous solution. The derivatives can not only kill cancer cells at a rate significantly higher than that by carboplatin, in particular, in the case of hepatoma cells, at a rate one to two times higher than that by carboplatin, but also produce little side effects such as vomit, baldness, decreases of leucocytes and platelets, and the like, which can be induced by administration of other chemotherapeutics. In the acute toxicity tests on mice, the lethal dose (LD50) of the present derivatives is about 300 mg/kg and 260 mg/kg body weight for a subcutaneous(sc) and an intraperitoneal(ip) administration, respectively. Therefore, the present derivatives are a novel class of cis-platium which can be widely used as anticancer agents.
CN101580466B Preparation method of sodium salt of pravastatin The invention discloses a preparation method of sodium salt of pravastatin, which comprises the following steps: adding inorganic alkaline or organic alkaline containing sodium ions as positive ions into organic solution containing the pravastatin until pH is more than 7 and obtaining sodium pravastatin; the organic solution containing the pravastatin comprises the pravastatin and first solvent, wherein the first solvent is selected from one or a plurality of methyl formate, n-propyl formate, isopropyl formate, n-butyl formate, methyl acetate, ethyl acetate, n-propyl acetate, isopropyl acetate, n-butyl acetate, sec-butyl acetate, isobutyl acetate and tert-butyl acetate.
WO2006030300A3 Processes for the preparation of olanzapine The invention relates to processes for the preparation of a crystalline polymorphic form of olanzapine. More particularly, it relates to the preparation of a crystalline polymorphic form of olanzapine designated as Form X and to pharmaceutical compositions that include the polymorphic Form X. The invention also relates to a process for the preparation of a methanol solvate of olanzapine and a process for using such solvate.
CN1970543A Synthesis and uses of serial ion liquid as candidate drug with anticancer activity The invention discloses an artificial synthetic new-typed anti-cancer drug with a series of ion liquid structure, whose structural formula is displayed in the formula (I), wherein R1,R2, R3,R4,R5,R6,X are defined as instruction; the compound inhibits tumour cell strongly such as Hela299,B16,SMMC-7721 and so on in the external anticancer activity test with effective density less than 10 mug/ml.
US20090274686 Nucleoside phosphonate derivatives The present invention discloses compounds of formula (I) or (II), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral/anti-proliferative compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral infection in a subject in need of such therapy with said compounds.
CN101926505A Caffeine electronic cigarette liquid The invention relates to caffeine electronic cigarette liquid, which mainly comprises 3-5%w/v of tobacco leaf extract, 5-10%w/v of pure water, 3-5%w/v of tobacco essence, 0.1-3%w/v of guarana extract with 5% in concentration, 0.2-1%w/v of stabilizer, 3-8%w/v of thickening agent and the balance of propylene glycol. The invention uses caffeine instead of nicotine; and the caffeine is an excitant for the central nervous system, and can increase the content of adenosine cyclophosphate (cAMP) in the cells. A small or medium amount of caffeine taken can excite the cerebral cortex, boost spirits of the people, enhance the attention, self-confidence, working efficiency and enthusiasm, shorten the time for selection and response and improve the recognition capability and instantaneously oral memory. In addition, the caffeine can promote synthesis and release of catecholamine, have positive effects to the cardiovascular system, promote gastric acid secretion, reduce the gallstone morbidity, and treat hemicrania and the like.
WO2007022102A3 Pentacyclic kinase inhibitors The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula: (I) wherein A, X, Y, Z, Ra, Rb, Rc, R1 , R2, R3 and m are defined herein.
US20100151041 Hypersaturated gas in liquid Dispersing a gas in a liquid to provide a mixture of saturated, supersaturated or hypersaturated solution to provide a suspension of bubbles containing gas therein.
WO2013007384A1 Use of lipoteichoic acid in the treatment of non-encapsulated cancer cells The present invention refers to the treatment of non-encapsulated cancer cells using lipoteichoic acid especially also to a treatment following directly a medical event that actually or possibly liberated non-encapsulated cancer-cells into the body like surgical removal of cancer tissue or a biopsy.
US7964186 modified adenovirus containing mutation in or lacks the virus associated RNA gene, modified HSV, vaccinia virus and parapoxvirus; Ras-activated pathway; neoplasm; immunosuppressant Methods for treating cell proliferative disorders by administering virus to proliferating cells having an activated Ras-pathway are disclosed. The virus is administered so that it ultimately directly contacts proliferating cells having an activated Ras-pathway. Proliferative disorders include but are not limited to neoplasms. The virus is selected from modified adenovirus, modified HSV, modified vaccinia virus and modified parapoxvirus orf virus. Also disclosed are methods for treating cell proliferative disorders by further administering an immunosuppressive agent.
WO2012028861A1 Pure erlotinib The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
US6911542 Pyrazino[1′,2′:1,6]pyrido[3,4b]indole derivatives Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
CN103330937A Monoclonal antibody-antigen binding segment-T-2 toxin conjugate The invention discloses a monoclonal antibody-antigen binding segment-T-2 toxin conjugate which is formed by connecting a monoclonal antibody-antigen binding segment with T-2 toxin by using one of a peptide chain, 1,4-butanediol diglycidyl ether, N-hydroxy succinimido-3-(2-pyrazolyl dithio)-propionate as a cross-linking agent. The invention further provides a preparation method of the monoclonal antibody-antigen binding segment-T-2 toxin conjugate and application of the monoclonal antibody-antigen binding segment-T-2 toxin conjugate in preparation of a targeted anti-tumor drug. According to the experiments, the conjugate disclosed by the invention has an obvious targeting performance for tumor tissues, and can be used for lowering the toxicity of the T-2 toxin and improving the inhibiting effect of the conjugate on the tumors.
EP1009414B1 Novel pharmaceutical composition comprising clindamycin and clotrimazol for the treatment of vaginal infections The invention relates to a new pharmaceutical composition containing clindamycin and clotrimazol used for the treatment of vaginal infections.
CN102144984A Easy-dissolution lamivudine tablet and preparation method thereof The invention relates to an easy-dissolution lamivudine tablet and a preparation method thereof. The lamivudine tablet comprises the following raw materials in parts by weight: 100 parts of lamivudine, 95-105 parts of microcrystalline cellulose, 5-8 parts of sodium carboxymethyl starch, 1.5-3 parts of magnesium stearate and 90-120 parts of 2% hydroxypropyl methylcellulose (E15) aqueous solution.
CN102600098A Glucosamine sustained release preparation and preparation method thereof A glucosamine sustained release preparation consists of various main and auxiliary raw materials including, by weight ratio, from 30 to 90% of glucosamine, from 1 to 50% of sustained release materials, from 1 to 20% of other auxiliary materials and from 3 to 5% of stomach soluble coating films. The glucosamine includes glucosamine hydrochloride, sulfate, phosphate, hydriodate and glucosamine mixture; the sustained release materials selectively include one or a combination of more than one of stearic acid, gelatin, glycerin monostearate, dextrin, methylcellulose, microcrystalline cellulose and ethyl cellulose; and the other auxiliary materials are selected from microcrystalline cellulose, silica, magnesium stearate and glycerin monostearate. The glucosamine is stably released by the aid of skeleton sustained release technology, the immunity of a patient suffering from osteoarthrosis is improved by means of supplementing the glucosamine, and pain of the patient is released. A preparation method is simple in process, fine in reproducibility and high in production efficiency, prepared tablets are released uniformly, and stability is good.
WO2009054001A1 A pharmaceutical composition and a process thereof A combination therapy is provided of an EGFR-inhibiting agent that competitively inhibits native EGF binding to the receptor and an immunosuppressant to treat a mammalian host, preferably human by administration of a therapeutically effective amount of the drug for the prophylaxis and/or treatment of tumors. The Immunosuppressant selected from the group comprising rapamycin, tacrolimus, everolimus, pimecrolimus in the free form or in the form of a pharmaceutically acceptable salt or solvates. Novel anti-EGFR drug-conjugates, and compositions optionally containing at least one pharmaceutically acceptable carrier for simultaneous use is also contemplated.
CN1868461A Tegaserod maleate oral prepn. An orally taken powder of Tijiaseluo maleate for treating constipation-type intestinovulnerable syndrome contains proportionally the superfine powder of Tijiaseluo maleate or its composition and the biologically acceptable auxiliary chosen from excipient, disintegrant and water-soluble polymer.
WO2009150118A3 Novel salts of (4-{[(5-{[(3-chlorophenyl)methyl]oxy}-2-methylphenyl)carbonyl]amino}-3-methylphenyl)acetic acid A series of novel salt forms of (4-{[(5-{[(3-chlorophenyl)methyl]oxy}-2-methylphenyl)carbonyl]amino}-3-methylphenyl)acetic acid, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
CN101224246A Preparing method of loquat leaf total triterpenic acid and antidiabetic use thereof The invention relates to a preparation method for triterpene acid of loquat leaf and the function of lowering the blood glucose. The preparation method comprises that dry loquat leaves are firstly extracted by ethanol or methanol with certain concentration, reclaimed in ethanol with low condensation for sedimentation, and centrifuged, precipitated and refluxing-decolorized with diatomite or done with chromatography with siliceous earth column, and then eluted with ethanol and reclaimed in condition of decompression and dried to obtain the triterpene acid of loquat leaf. Total content of ursolic acid, oleanolic acid, maslinic acid, corosolic acid and tormentic acid in the triterpene acid reaches more than 50 percent (by weight), wherein, the content of the tormentic acid is to be 10-30 percent, the maslinic acid 4-20 percent, the corosolic acid 5-20 percent, the oleanolic acid 1-10 percent and the ursolic acid 5-20 percent. The triterpene acid of loquat leaf prepared by the invention can be used for curing diabetes mellitus or preparing pharmaceutic preparations used for treating diabetes mellitus and diabetic complication.
US6939897 Method and composition for inhibiting arteriosclerosis The present invention has for its object to provide a method and a composition for achieving a more efficient recovery of the antioxidant activity of plasma LDL, or even augmentation thereof, which has been depressed by the use of an antihyperlipidemic or cholesterol-lowering drug to thereby insure a potentiated antiarteriosclerotic efficacy. A method for inhibiting arteriosclerosis, which comprises using a combination of a cholesterol-lowering agent and a reduced coenzyme Q10 represented by the following formula (1), and a composition for inhibiting arteriosclerosis containing both a cholesterol-lowering agent and said reduced coenzyme Q10.
CN102379881A Application of 4-hydroxy salicylamide in preparing medicament for preventing and treating hepatitis and resisting tumor The invention provides novel application of 4-hydroxy salicylamide in the field of pharmacy. The compound is an inhibitor of ribonucleotide reductase (RR), and can achieve the aims of inhibiting replication of HBV and treating hepatitis, in particular the hepatitis B by inhibiting activity of RR enzyme to block synthesis of dNTPs (deoxynucleotide triphosphates) required by hepatitis B virus (HBV)replication, achieve the aim of preventing and treating liver cancer by inhibiting the activity of RR of liver cancer cells, including the RR activity activated by HBV to inhibit proliferation of liver cancer cells, and achieve the aim of treating various tumors by inhibiting the RR. The 4-hydroxy salicylamide can be used for preventing and treating hepatitis B, liver cancer, oropharyngeal epithelioma, colorectal cancer, ovarian cancer, non-small cell lung cancer, chronic myeloid leukemia and other tumors, and has important application prospect.
US7507728 for the treatment of cognitive disorders, anxiety, schizophrenia, and Alzheimer's disease; 10-chloro-9H-imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine; ligands; GABA A alpha 5 receptor inhibitors; halogenation The invention relates to halogen substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1, R2, R3, R4 and n are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used as a cognitive enhancer or for the treatment of cognitive disorders, anxiety, Alzheimer's disease and schizophrenia.
CN101062182A Medicine made from root of dahuriae angelica, atractylodes and so on for treating snakebite Disclosed is a medicament for treating snake bites, which is prepared from atractylodes rhizome, dahurian angelica root, centipede 2 pieces, silver flower, capsule of weeping forsythia, ledebouriella root, scrophularia root and pollen.
CN101574461A Drug composition for reducing blood sugar and blood fat and curing diabetes The invention relates to a drug composition for reducing blood sugar and blood fat and curing diabetes. The drug composition comprises common yam rhizome, golden thread, composite vitamin B, vitamin E, and trace elements of zinc, selenium, chromium and molybdenum. The drug composition is applicable to the crowds with high blood sugar, high blood fat and diabetes, is very effective in reducing blood sugar and blood fat and curing diabetes and can be applied for a long time or applied according to the course of the treatment.
US20080045582 ENA-78 Gene Polymorphisms and Protein Concentrations as Diagnostic and Prognostic Tools The invention concerns polymorphisms in the CXCL5 gene and the concentration of epithelial neutrophil activating peptide (ENA-78) in patients. The invention also pertains to methods and systems for detecting such polymorphisms. The invention further relates to the use of such methods and systems in the diagnosis, prognosis, and treatment selection for inflammatory disorders associated with elevated ENA-78 concentrations.
US20090093669 Magnetophoresis apparatus and method of use A method and apparatus for administering drugs through a dermal or mucosal layer such that the treatment device may be applied to the mammal for the transdermal or transmucosal administration of various drugs, pharmaceuticals, salts and prodrugs thereof is taught herein. The magnetic device has at least one magnet to provide an effective magnetic sphere of influence of the magnetic field at the desired site of action. The tissue-permeable drug formulation is positioned on the site of action and the magnetic device is positioned adjacent to tissue-permeable drug formulation wherein the magnetic sphere of influence of the magnetic field moves the drug through the dermal or mucosal layer by interaction with the magnetic moment (induced or permanent) of the drug sufficient to increase the movement of the drug beyond the movement caused by diffusion alone.
CN102600088A Injection lansoprazole medicine composition and preparation method thereof The invention relates to an injection lansoprazole medicine composition which comprises the following components in parts by weight: 3 parts of lansoprazole, 5-15 parts of poloxamer 188 and 10 parts of mannitol. A preparation method comprises the following steps of: adding injection water in the lansoprazole, stirring to ensure that the lansoprazole is dispersed, regulating the pH to be 10.55-10.60, stirring to ensure that the lansoprazole is dissolved, adding the mannitol, stirring and dissolving to obtain a solution I; dissolving the poloxamer 188 with injection water, regulating the pH to be 10.80-10.90 to obtain a solution II; mixing the solution I and the solution II, regulating the pH to be 10.80-11.2, adding injection water to obtain a medicine solution; and adding active carbon inthe medicine solution, stirring, removing carbon through filtering, filtering and sterilizing, drying through freezing to obtain lansoprazole freeze-dried injection. The injection lansoprazole medicine composition prepared by adopting the invention has good quality and high stability.
US20090018105 Means and Methods for the Treatment and Prevention of Allergic Diseases The present invention relates of the use of certain inner ionic (zwitter ionic) phospholipids, phosphonolipids and phosphate derivatives for the preparation of a pharmaceutical composition for the treatment, prevention and/or amelioration of an immunological disorder related to mast cell sensitization. Preferred in this context are edelfosine and miltefosine. In a particularly preferred embodiment, the present invention relates to the use of miltefosine for the preparation of a pharmaceutical composition for the treatment, prevention and/or amelioration of allergic diseases, in particular acute hyperallergic diseases, like asthma.
EP2231185A1 Methods and compositions for treating liquid tumors The application relates to a method of using compositions having anti-alpha- 4 integrin and/or anti- alpha-9 integrin activity to inhibit liquid tumor growth, malignancies thereof and/or development of metastases thereof that involve expression of an alpha-4 integrin and/or alpha-9 integrin. Pharmaceutical compositions and combination therapies (for example, with chemotherapies) for the inhibition of liquid tumor growth, malignancies thereof and/or development of metastases thereof are also provided.
CN101074200A Aspartic acid salt of O-demethyl-Venlafacin A 0-demethyl-Effexor salt, aspartic acid salt and its medicinal composition are disclosed.
CN103494786A Medicinal composition containing moxifloxacin hydrochloride The invention relates to the technical field of pharmaceutical preparations, in particular to moxifloxacin hydrochloride dispersible tablets and preparation method thereof. The dissolution problem of moxifloxacin hydrochloride can be significantly improved by adding a proper amount of potassium bicarbonate or sodium bicarbonate to a formula of the dispersible tablets. After moxifloxacin granules are coated with Eudragit E100, coatings of the granules never break due to environmental pH; accordingly, adverse bitterness of moxifloxacin can be covered effectively, and administration compliance of patients is improved. In addition, granules of the medicinal composition are dry, the coating drying process can be completed in a fluidized bed, and the medicinal composition is applicable to industrial production.
WO2012148140A2 Imidazole-based alkaloid derivatives which have angiogenesis inhibition and antioxidant effects and production method thereof The present invention relates to imidazole-based alkaloid derivatives represented by formula (1) in the description, pharmaceutically acceptable salts, hydrates, solvates, isomers, prodrugs and a preparation method, thereof, and a pharmaceutical composition containing same which has angiogenesis inhibition and antioxidant effects. In the formula, L, M, m, X, Y, R1 and R2 are as defined in the description.
US20050119345 2-Amino-3-alkoxy-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives; effective for treating and preventing psychiatric disorders such as schizophrenia, anxiety, bipolar disorder and epilepsy, neurological diseases such as drug dependence, Alzheimer's disease, Huntington's chorea An antidepressant comprising, as an active ingredient, a compound having an antagonistic effect on group II metabotropic glutamate receptors, as well as a 2-amino-3-alkoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative of Formula [I]: [wherein R1 and R2, which may be the same or different, each represent a hydroxyl group, a C1-10 alkoxy group, etc.; R3 represents a C1-10 acyl group, a C1-6 alkoxy-C1-6 acyl group, etc.; and R4 and R5, which may be the same or different, each represent a hydrogen atom, a C1-10 alkyl group, etc.] or a pharmaceutically acceptable salt or hydrate thereof.
CN102127079A Pyrrolo-pyrazin-carboline diketone compounds and preparation method and applications thereof The invention discloses pyrrolo-pyrazin-carboline diketone compounds, namely 4-(1R,3S,2'S)a-d and 4-(1S,3S,2'S)a-d, and a preparation method and applications thereof. The compounds inhibit the urokinase-type plasminogen activator receptor and then inhibit the in-vitro and in-vivo thrombolytic activities of urokinase, thus the compounds have the function of promoting thrombosis on the rat thrombosis model. Threrefore, the pyrrolo-pyrazin-carboline diketone compounds provided by the invention have clinical application prospect when used as coagulant.
WO2013156225A1 Optimizing ungual treatment by quantitative autoradiography A method for optimizing ungual treatment includes (a) providing a nail having at least two spaced apart holes formed from a surface thereof and extending into the nail, and (b) topically applying a radiolabeled pharmaceutical composition to the nail. At least a portion of the composition is received in the at least two holes. The method also includes (c) sectioning a portion of the nail proximate the at least two holes into a plurality of sections, (d)determining, for each of the plurality of sections, a concentration of radio activity in the section as a function of position with respect to the at least two holes, and (e) optimizing a spacing between the at least two holes based at least partially on the determinations in step (d). A method of ungual treatment using the optimized spacing is also described.
US8598146 Methods for identifying modulators of protein kinase C-epsilon (PKCε) and method of treatment of aberrant glucose metabolism associated therewith The present invention provides novel cell-based and animal-based assays for determining antagonists of PKCε and uses of the isolated antagonist compounds for modulating insulin clearance and secretion. The invention also provides novel animals and cells such as animals and cells suitable for use in the assays.
EP1722856A1 Use of 2-methylene-19-nor-20(s)-1alpha,25-dihydroxyvitamin d3 for the prophylaxis of bone diseases This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1α,25, dihydroxyitamin D3. This compound is characterized by high bone calcium mobilization activity demonstrating preferential activity on bone. This results in a novel therapeutic agent for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis. This compound also increases both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements, as well as use by normal subjects when high bone mass is desired.
WO2007103427A2 Medical use of bilirubin and its structural analogues Formulations and methods for preventing, inhibiting or controlling metabolic disorder, age-related disease and acute inflammations have been developed. The compositions comprise of bilirubins, bilirubin derivatives, their tetrapyrrolic analogues, tripyrroles, and dipyrroles. The compositions can be administered as a dosage form for oral ingestion, injection, suppository, or topical application. The effective amount of the compound is typically from 0.001 - 100 mg/kg body weight, preferably in the range from 0.01 - 50 mg/kg body weight, and most preferably from 0.05 - 10 mg/kg body weight. Examples demonstrate the efficacy of the compounds in both in vitro and in vivo tests.
US7629349 Parkinson's disease; antidepressants; cognition activators; analgesics; brain disorders; drug combination Pharmaceutical compositions and their uses comprising compounds of formula (I): wherein: R1 is selected from: alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR6R7, NR5COR6, NR5CONR6R7, NR5CO2R8, and NR5SO2R8; R2 is a heteroaryl attached via an unsaturated ring carbon of said heteroaryl group; R3 is selected from: H, alkyl, halogen, OR5, SR5, and NR6R7; R4 is selected from: H, acyclic alkyl, CONR6R7, CONR5NR6R7, COR6, CO2R8, and SO2R8; R5, R6, and R7 are independently selected from: H, alkyl, and aryl, or where R6 and R7 are in an NR6R7 group, R6 and R7 may be linked to form a hetero cyclic group, or where R5, R6 and R7 are in a (CONR5NR6R7) group, R5 and R6 may be linked to form a heterocyclic group; and R8 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof.
CN101433529A Glycyrrhizic acid transdermal formulation and preparation technique thereof The invention discloses a glycyrrhizic acid percutaneous preparation, which comprises the following compositions by weight portion: 0.1 to 50 portions of glycyrrhizic acid or salt thereof, and 0.5 to 10 portions of percutaneous accelerating agent or a percutaneous absorption carrier. Absorption of the medicine is affected by the pH value in alimentary canal, moving time of foods and the medicine in the intestinal canal, and other complicated factors; the first-pass effect of the medicine in the liver can be avoided; the speed of administration can be continuously controlled; and an administration position of the medicine is on the body surface, so the administration can be interrupted conveniently. The percutaneous preparation is an external use preparation, has the advantages of convenient administration, strong target property, non skin irritation, simple and convenient preparation and the like. Compared with an oral preparation and an injection, the percutaneous preparation can be taken more safely and can overcome side effects of the oral preparation and the injection. Due to the characteristic of high concentration of local administration, the percutaneous preparation is particularly applicable to dermal diseases.
CN101601844A Preparation method of ointment for clearing infantile tetanus neonatorium The invention discloses a preparation method of an ointment for clearing the infantile tetanus neonatorium. The infantile tetanus neonatorium can be eliminated within hours by using the method. The method is realized by adopting the following technical scheme that: ginger, welsh onion and radish seeds are respectively smashed into broken paste, salt is fried for 5-10 minutes at 50-60 DEG C and then respectively added in the broken paste and then evenly stirred for 5-30 minutes, and then the two kinds of the broken pastes are mixed together to be added with vinegar to stirring for 10 minutes to obtain the finished external medical ointment.
US20090233975 Hair resiliency/body improver and hair cosmetic A hair resiliency and body improver comprising as the active ingredient thereof one or more types of compounds selected from the group consisting of 2-aminothiazole derivatives represented by the following general formula (1) or 3-aminoisoxazole derivatives represented by the following general formula (2), and pharmaceutically acceptable salts thereof: (wherein, R1, R2, R3, R4, n and m are as defined in the description).
EP2238977A2 Skin cleaning products Formulation (I) for a foaming skin cream, comprises an aqueous emulsion (Ia) and a propellant, where (Ia) comprises urea and hyaluronic acid, at least one free fatty acid and at least two emulsifiers, where the hyaluronic acid exhibits a molecular weight of at least 1 x 10 5> Da. Independent claims are included for: (1) a formulation (II) for a foaming skin cream, comprising an aqueous emulsion (IIa) and a propellant, where the emulsion comprises urea and carbohydrate mixture that is obtained from natural source, at least one free fatty acid and at least two emulsifiers; (2) a formulation (III) for a foaming skin cream, comprising an aqueous emulsion (IIIa) and a propellant, where the emulsion comprises at least free fatty acid and at least two emulsifiers and the pH is adjusted to 5.5-8 with potassium hydroxide; (3) a foam skin cream that is obtained from the formulation; (4) a day and night skin care set, comprising a day skin care composition and a night skin care composition, where the day skin care composition is the foaming skin cream that comprises at least one free fatty acid and at least two emulsifier, where the night skin care composition comprises an additional active substance or a higher wt.%-portion of an active substance or another active substance as the day skin care composition, where the active substance is a lipid substance and/or its hydrates; and (5) a method for treating dermatosis comprising applying the formulation on the skin. - ACTIVITY : Antiinflammatory; Dermatological; Antipsoriatic. - MECHANISM OF ACTION : None given.
CA2446828C Adenosine a1 receptor antagonists for treating hypoxia-induced learning and memory impairment The invention provides therapeutic methods and compositions comprising adenosine A1 antagonists for treating memory loss produced by reversible transient hypoxia and associated synaptic dysfunction.
CN1739546A Use of skullcap aglycone and baicalin in preparing antitumor medicine The present invention relates to the new medicinal use of skullcap aglycone and baicalin, and is especially the use of skullcap aglycone and baicalin in preparing antitumor medicine.
WO2014033480A1 Histamine 4 receptor partial agonists, inverse agonists or antagonists for use|in treating non-autoimmune uveitis The invention provides a compound which is a histamine 4 receptor antagonist, partial agonist or inverse agonist, for use in the treatment of non-autoimmune uveitis. The compound preferably has a structural core comprising a substituted pyrimidine group, such as an aminopyrimidine, diaminopyrimidine or triaminopyrimidine group, a thienopyrimidine, a furopyrimidine, a benzimidazole, an aryl or heteroaryl-fused pyrimidine, an indole, a bicyclic heteroaryl-substituted imidazole or a quinazoline group.
WO2011084898A3 Enhanced bone healing The combined use — whether by adsorption or covalent linkage — of Melatonin adjacent any bone implant or graft, preferably any calcium- and oxide-containing artificial bone graft material, and more preferably a calcium aluminate composition. Alternatively, the bone graft or implant material may be used as a scaffold for tissue engineering.
CA2190765C Novel potent inducers of terminal differentiation and methods of use thereof The present invention provides the compound having structure (I), wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiazoleamino group; when R1 and R2 are different, R1 = R3-N-R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
US20080221169 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels; brain trauma, head trauma, eye disorder, pulmonary disorder, lung disease, vascular disease, kidney disease, heavy metal toxicity, Alzheimer's disease, tumor, and cancer Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
CN101190922B Cephalosporin derivative The invention relates to compounds of novel cephalosporin derivatives as well as pharmaceutically acceptable salts, easy hydrolysis ester, isomer, hydrates and hydrates of salts or esters thereof shown in the general formula (1), wherein, R<1>, R<2>, R<3>, R<4>, R<5> and R<6> are defined as the instruction. The invention also relates to the preparation methods of the compounds, medical composition, which contains the compounds, and the application of the compounds in preparation of drugs, which are used for curing and/or preventing diseases caused by viral infection, and pertains to the fieldof medical technologies.
WO2012094081A2 System and method for identifying and applying peripheral treatment mechanisms for disease A method and system for the identification and application of biological targets for peripheral treatment of diseases. Existing cellular mechanisms or pathways are exploited to identify novel genes or other molecule candidates that will be used to treat disease via a peripheral treatment system. Using the method, a novel Alzheimer's disease target is identified and used to treat an animal Alzheimer's disease model via peripheral expression of that target.
WO2008081399A3 2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
US20070287688 Pharmaceutical Compositions for Topical Application Compounds of Formula I are useful as skin penetration enhancing agents: (I) wherein: R represents a linear, saturated or unsaturated, substituted or unsubstituted hydrocarbyl radical; and X represents a —(CO)O—, —O(CO)—, C═O, CONH, O, NHCONH, S, or S═O radical. Compositions and methods using these compounds are also described.
US7650733 Method and apparatus for loading a container with a product There is provided a method of loading a container with a defined quantity of product which comprises the steps of a) closing off a perforation (12 a , 12 b) in a perforated plate (10); b) directing powder (30) into said closed-off perforation; and c) transferring the contents of the perforation to said container.
WO2010111759A1 Stabiliser-free pharmaceutical compositions of tetrahydrolipstatin The present invention relates to a composition and pharmaceutical formulation comprising a mixture of an effective amount of powders or granulates of a compound derived from leucine and at least one pharmaceutically acceptable excipient used as the carrier. In particular, the main feature of the formulation and composition that form the subject matter of the present invention is that they are devoid of stabilisers and can be included in any conventional pharmaceutical formulation for oral administration.
US20090149530 Antiinfective Flavonol Compounds and Methods of Use Thereof In one aspect of the invention, the antiinfective agents are flavonol compounds of the represented by formula I: Another aspect of the invention is a method for treating an infection in a subject by administering the compounds of Formula I to the subject.
WO2007091950A1 Benzimidazoles and imidazopyridines useful in the treatment of diseases or disorders associated with cannabinoid receptor 2 (cb2) such as pain This invention relates to novel benzimidazoles and imidazopyridines having the structural of formula I below and their pharmaceutically acceptable salts, tautomers or in vivo -hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide treatments of CB2 associated disorders.
US20120322885 Materials and Methods for Improving Alcohol Metabolism and Alleviating the Effects of Hangovers The subject invention provides materials and methods for improving alcohol metabolism in animals. In a preferred embodiment, the invention provides methods for increasing the ability of people to consume alcohol while reducing hangovers or other effects of intoxication. Specifically exemplified herein is the use of a cysteamine compound to reduce the adverse effects of alcohol consumption. For example, the undesirable and unpleasant symptoms association with hangovers can be reduced through consumption, according to the subject invention, of cysteamine hydrochloride.
WO2012006563A2 Novel daidzein analogs as treatment for cancer Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.
US7247618 Methods for inhibiting macrophage colony stimulating factor and c-FMS-dependent cell signaling Described herein are methods of inhibiting M-CSF activity, and, in particular, M-CSF/c-fms dependent cell signaling. In a first embodiment of the invention, one administers to a mammal viral vectors that deliver genes experessing antisense c-fms RNA; in a second embodiment, one induces in vivo production of a high-affinity soluble c-fms protein that competes for non-bound M-CSF; in a third embodiment, one administers a ribozyme-viral vector against c-fms mRNA; and in a fourth embodiment, one administers oligodeoxynucleotides that inhibit expression of c-fms gene product. The methods may be used to treat any disease in which M-CSF activity plays a role, and are particularly effective in treating and preventing atherosclerosis. Embodiments of the present invention are directed primarily, but not exclusively, to a method for treating and preventing cardiovascular disease by inhibiting receptors to M-CSF. Other embodiments of the present invention include any and all biologic and/or pathobiologic phenomena mediated in whole or in part by M-CSF signaling through its receptor. Pathobiologic phenomena include, but are not limited to, disease entities such as osteoporosis, Alzheimer's disease, diabetes mellitus (Type 1 and/or Type 2), infectious diseases, cancer, and inherited disorders characterized by defects in one or more components in the M-CSF signaling pathway.
US20130059859 Predictive biomarkers for pi3k/akt kinase pathway inhibitor efficacy A method of predicting the sensitivity of tumor cell growth to inhibition by a PI3K/AKT kinase pathway inhibitor, comprising: determining the localization profile of FOXO3a in a tumor cell, wherein a cytoplasmic localization profile of FOXO3a correlates with sensitivity to inhibition by a PI3K/AKT kinase inhibitor and a nuclear localization profile of FOXO3a correlates with resistance to inhibition by a PI3K/AKT kinase inhibitor.
CN102911188A Sulfur-containing diindolyl diketopiperazine compounds and application thereof in preparing antineoplastic drugs The invention discloses sulfur-containing diindolyl diketopiperazine compounds and application thereof in preparing antineoplastic drugs. Five sulfur-containing diindolyl diketopiperazine compounds are separated from the marine eumycete Acrostalagmus luteoalbus SCSIO F457. The structural formula is disclosed as Formula (I). The compounds 1-5 have strong growth inhibition action on human central nervous system cancer cell SF-268, human breast cancer cell MCF-7, human large-cell lung cancer cell NCI-H460 and human liver cancer cell HepG2, have better effects than the positive control drug cisplatin on the whole, and can be used for preparing antineoplastic drugs. Therefore, the invention provides alternate compounds for developing new antineoplastic drugs, and has important meanings for developing Chinese marine drug resources. Formula (I).
CN102846722A Pharmaceutical composition for treating urinary calculus The invention relates to a pharmaceutical composition for treating urinary calculus and is characterized in that the pharmaceutical composition is a decoction prepared from the following raw materials of: by weight, 30-60 parts of desmodium, 8-10 parts of chicken's gizzard membrane, 8-10 parts of akebia stem, 8-10 parts of cyathula root,8-10 parts of dianthus superbus, 8-10 parts of Plantain seed, 14-16 parts of talcum, 3-5 parts of amber and 9-15 parts of ural licorice root tip. The medicine provided by the invention can be made into a decoction which can be accepted in clinic. One dose of the medicine is taken for each day, and patients with acute ache can take two doses. The pharmaceutical composition provided by the invention has simple and reasonable compatibility and has a significant curative effect of treating urinary calculus.
CN101015604A Heat clearing powder for treating chicken egg drop syndrome in summer and its preparing process The invention relates to a heat-clearing powder for treating low egg-laying syndrome in summer and its preparing process, which is prepared from the following constituents (by weight portions) through mixing homogeneously: dyers woad leaf 48-72g, radix isatidis 48-72g, calcium sulphate 48-72g, rhubarb horsetails 24-36g, compound of glauber-salt and liquorice 24-36g. The preparing process consists of disintegrating the raw materials, passing through 20-80 mesh sieves, and mixing homogeneously.
US20090048187 Chemopreventive, Anticancer and Anti-Inflammatory Effects of Pinoresinol-Rich Olives The present invention relates to a composition and method for preventing and treating cancer and modulating cell proliferation using compositions extracted from pinoresinol-rich Olea europaea Caiazzana olives. The present invention provides contacting one or more cells with a pharmaceutical effective amount of a polyphenolic composition isolated from Olea europaea Caiazzana olives. The polyphenolic composition includes one or more polyphenolic compounds extracted from Olea europaea Caiazzana olives.
WO2011000565A1 Eltoprazine for the treatment of anxiety The present invention relates to the treatment of an individual afflicted with certain forms of anxiety, the instant treatment comprising administering to the individual an effective amount of eltoprazine or a pharmaceutically acceptable salt thereof.
US7714015 Method and composition for treating sunburned skin The present invention relates to a method and composition for treating sunburned skin. The present invention provides a method and composition for applying a mixture of indomethacin and moisturizing lotion topically to sunburned skin. The composition includes a mixture having substantially 100 milligrams of indomethacin per 30 cc of moisturizing lotion. The moisturizing lotion is marketed under the trade name Cetaphil® and includes the following ingredients: purified water, glycerin, hydrogenated polyisobutene, cetearyl alcohol (and) ceteareth-20, macadamia nut oil, dimethicone, tocopheryl acetate, stearoxytrimethylsilane (and) stearyl alcohol, panthenol, farnesol, benzyl alcohol, phenoxyethanol, acrylates/C10-30 alkyl acrylate crosspolymer, sodium hydroxide, and citric acid. It is theorized that the Cetaphil® provides certain pH and viscosity levels which allow for the stabilization and solubilation of the indomethacin within the Cetaphil®.
US7220403 Pharmaceutical formulation of fluticasone propionate There is provided according to the invention a pharmaceutical aerosol formulation which comprises: (i) fluticasone propionate and (ii) a hydrofluoroalkane (HFA) propellant, characterised in that the fluticasone propionate is completely dissolved in the formulation. The invention also provided canisters containing the formulation and uses thereof.
WO2006095870A1 Photosensitizer, protein-cleaving agent, method of cleaving protein, sugar molecule-cleaving agent, method of cleaving sugar molecule, and photodynamic therapeutic agent [PROBLEMS] To provide a novel photosensitizer, methods of cleaving a protein and cleaving a sugar molecule with light irradiation, and a protein-cleaving agent and sugar molecule-cleaving agent for use in these methods. [MEANS FOR SOLVING PROBLEMS] A compound represented by the following general formula (I) or a salt thereof generates active oxygen upon light irradiation and functions to cleave a protein and sugar molecules. The compound or salt is hence useful in applications such as a photosensitizer, protein-cleaving agent, sugar molecule-cleaving agent, and photodynamic therapeutic agent. [Chemical formula 1] (I) (In the formula, R1 to R8 each is hydrogen or a hydroxylated substituent, provided that at least one of R1 to R8 is a hydroxylated substituent.)
CN102432555A 1, 2, 3-triazole-4 (5) carboxamide compound and application thereof The invention provides a 1, 2, 3-triazole-4 (5) carboxamide compound with a structure in formula (I), or its pharmaceutically acceptable salt or stereoisomer or prodrug molecule, and their application in preparing medicaments for influenza prevention and treatment, as well as pharmaceutical compositions for influenza prevention and treatment with the compound as a pharmaceutical active component. The invention researches in vitro antiviral activity of the compound and its inhibition on entrance of virus nucleoprotein into a host nucleus. And results show that, the compound of the invention can obviously block virus nucleoprotein from entering a host nucleus and presents substantial activity in inhibiting an influenza virus, thus providing a new medicament choice for clinical treatment of influenza.
CN103570614A Pyridine-2-hydrazide derivatives, preparation method, drug compositions and uses thereof The present invention relates to pyridine-2-hydrazide derivatives represented by formulas I and II, pharmaceutical salts, hydrates and solvates thereof, a preparation method of the pyridine-2-hydrazide derivative, drug compositions containing one or a plurality of the compounds, and uses of the compounds in treatment of protein kinase related diseases such as immune disorders and tumor diseases.
US6958241 Liposomes with outer surfaces having an affinity moiety that binds to a biological therapy target surface, and a hydrophilic polymer coating reversibly conjugated to said moiety; e.g. polymyxin B conjugate liposome for septic shock A method of liposome-based therapy for a mammalian subject is disclosed. The method uses liposomes with outer surfaces that contain an affinity moiety effective to bind specifically to a biological surface at which the therapy is aimed, and a hydrophilic polymer coating effective to shield the affinity moiety from interaction with the target surface. The hydrophilic polymer coating is made up of polymer chains covalently linked to surface lipid components in the liposomes through releasable linkages. After a desired liposome biodistribution is achieved, a releasing agent is administered to cause cleaving of a substantial portion of the releasable linkages in the liposomes, to expose the affinity agent to the target surface.
WO2008032696A1 Preventive or therapeutic agent for respiratory disease An agent for suppressing both progression and acute exacerbation of decreased respiratory function with age in respiratory disease, comprising a compound having a squalene synthase inhibitory action and represented by the formula: (I) (wherein R1 represents a hydrogen atom or a hydrocarbon group which may be substituted; R2 and R3 are the same or different and represent a hydrogen atom, a hydrocarbon group which may be substituted or the like; X' represents a carboxyl group which may be esterified, a carbamoyl group which may be substituted, a hydroxy group which may be substituted, an amino group which may be substituted, or a group constituted by a heterocyclic residue which has a deprotonatable hydrogen atom and may be substituted; the ring A represents a benzene ring or a heterocyclic ring which may be substituted; the ring J' represents a 7- or 8-membered heterocyclic ring containing 3 or less heteroatoms as ring constituent atoms, and the ring J' may further have a substituent other than R1, R2, R3 and X').
WO2009097113A3 Oxazole and thiazole compounds as b-catenin modulators and uses thereof A series of oxazole and thiazole compounds are shown herein to be small molecule inhibitors of the Wnt pathway that specifically target the activity of the stabilized pool of β-cat oxazole and thiazole compounds are disclosed that have a formula represented by the following.The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cancer, and others.
CN101912613B Taste masking preparation The invention relates to an oral taste masking preparation and a preparation method thereof. The invention is characterized in that an auxiliary material which expands with water is added in the preparation process, owning to the hydro-expansiveness of the auxiliary material, a film is formed in the outer layer of a medicine, thus enabling the medicine to form a shape similar to an frog egg, delaying the contact time between the medicine and body liquid and masking the taste; and an preparation formula and an preparation process of the original product do not need to be changed, and a production spot and a device do not need to be reformed. The preparation method is simple and convenient, and industrialization can be easily achieved.
CN1813691A Decanoyl acetaldehyde compound and its medicinal composition The present invention relates to a compound which contains decanoyl acetaldehyde and has storage stability and its medicinal composition. Said compound is made up by uniformly dispersing decanoyl acetaldehyde into lipa medium, the mass percentage of decanoyl acetaldehyde contained in said compound is 0.2%-10%, and the mass percentage of lipa contained in the compound is 20%-99.8%. Said compound can be made into medicinal composition after other medicinal auxiliary materials are added in said compound, said medicinal composition can be made into capsule, dripping pills, soft capsule and tablet preparation.
US20080089845 optimizing therapeutic efficacy for treatment of anxiety, depression, pain, or a metabolic disorder by increasing or decreasing a dose of a fatty amide ( oleoylethanolamide or palmitoylethanolamide) hydrolase inhibitor according to a patient's fatty amide levels by administering a carbamate derivative Described herein is a method for determining an effective dose of a composition for inhibiting fatty acid amide hydrolase activity in vivo, by first administering to a subject a dose of a test composition, and subsequently assessing if the level of a fatty acid amide in the subject increases. Also described, is a method for optimizing therapeutic efficacy for treatment of anxiety, depression, pain, or a metabolic disorder by increasing or decreasing a dose of a fatty amide hydrolase inhibitor according to a patient's fatty acid amide levels. In addition, pharmaceutical compositions are described, which contain fatty acid amide hydrolase inhibitors effective for increasing a FAA level in a patient.
WO2007064993A3 Bicyclic protein kinase inhibitors Compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit protein kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
CN1742810A Medicine composition for treating malaria The present invention relates to a medicine composition for curing malaria. Said medicine composition contains (by weight portion) 8-15 portions of licorice, 8-15 portions of kansui root, 8-15 portions of mylabris, 5-7 portions of white pepper, 1-2 portions of musk and 1-2 portions of borneol. Said invention also provides its preparation method and its application method.
US20110002844 Stabilization of macromolecular membranes Disclosed are stabilized polymersomes having layer structures. Such stabilized polymersomes are, in some embodiments, biocompatible, and are capable of enhanced, sustained release of agents. Also disclosed are related methods for synthesizing such stabilized polymersomes and methods for using such polymersomes for delivery of therapeutic, imaging, and various other agents.
WO2009075776A1 Process for the preparation of retapamulin and its intermediates Processes for preparing tropine derivatives of the following Formula B are provided where LG represents a leaving group. The tropine derivatives may be used to prepare Retapamulin, preferably in substantially pure form. Also provided are processes for preparing Retapamulin comprising combining a base, tropine thiol in a free base or salt form, an organic solvent, and a pleuromutilin derivative of Formula A.
EP2599866A1 Novel nucleic acid having adjuvant activity and use thereof The disclosed nucleic acid at least containing a single-stranded DNA to be delivered to endosomes of dendritic cells and a double-stranded RNA capable of activating TLR3 can be delivered to endosomal TLR3 and has a strong adjuvanticity with few side effects, and therefore is useful as an active ingredient of immunostimulants, vaccine adjuvants, cancer therapeutic agents and the like.
CN103610757A Injection for clearing heat, reducing phlegm and detoxifying The invention relates to an injection for clearing heat, reducing phlegm and detoxifying. The injection comprises active substances, propylene glycol and water for injection. The active substances are prepared from the following materials: bear gall powder or ursodesoxycholic acid, cornu gorais, scutellaria baicalensis, honeysuckle and fructus forsythiae. The invention also relates to a preparation method of the injection and a pharmaceutical use thereof. The injection provided by the invention can be used for clearing heat, reducing phlegm and detoxifying; the injection can be applied to wind-warm lung-heat disease which belongs to phlegm-heat obstructing lung syndrome, and can be used for treating fever, cough, expectoration and un-comfort, swollen sore throat, thirst, reddened tongue and yellow tongue coating; the injection can be used for patients suffering early-stage pneumonia, acute bronchitis, acute attack of chronic bronchitis and upper respiratory infection with the previous syndromes.
US8715922 Virus causing respiratory tract illness in susceptible mammals The invention relates to the field of virology. The invention provides an isolated essentially mammalian negative-sense single stranded RNA virus (MPV) within the subfamily Pneumovirinae of the family Paramyxoviridae and identifiable as phylogenetically corresponding to the genus Metapneumovirus and components thereof.
EP2571881A1 Pyrrolopyrazine derivatives as syk and jak inhibitors The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables Q and R1 and R2 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
US20100255112 Efficient Nuclear Delivery of Antisense Oligonucleotides or siRNA In Vitro and In Vivo by Nano-Transforming Polymersomes Provided is a biocompatible polyethylene oxide (PEO)-based polymersome system for the delivery of oligonucleotides, including antisense RNA, siRNA and RNAi, to a cell or tissue target, and method of use therefore, wherein the method comprises encapsulating the oligonucleotide in a biodegradable neutral, nano-transforming polymersome delivery vehicle and delivering the encapsulated oligonucleotide to the cell or tissue target in vitro or in vivo, particularly for treating a disease, such cancer or cellular hyperproliferation. The degradable polymersome, and the oligonucleotides stably encapsulated therein are taken up passively by cells and delivered into endolysosomes, wherein the polymersomes decompose at a known rate at a known pH, thereby releasing encapsulated oligonucleotides in a controlled manner within the cell and facilitating delivery of antisense oligonucleotide or siRNA or RNAi into the nucleus of the cell target.
EP2415473A1 Oral Care Compositions Containing Combinations of Anti-Bacterial and Host-Response Modulating Agents The present invention encompasses topical oral care compositions comprising the combination of an anti-bacterial agent with an anti-inflammatory agent in an orally acceptable carrier for effective treatment and prevention of bacteria-mediated diseases and conditions in the oral cavity and for modulating host reaction to bacterial pathogens present in the oral cavity and to the toxins, endotoxins, inflammatory cytokines and mediators released by or prompted by these pathogens. The benefits of the present compositions and methods extend beyond treating and preventing bacterial infections in the oral cavity to promoting whole body or systemic health.
CN101912379A Application of methyl ketone compounds The invention relates to an application of fatty group methyl ketone compounds. The fatty group methyl ketone compounds with the structure disclosed as formula I can be used for preparing medicines for treating bacterial acute infection diseases. In the formula I, n is a whole number of 4-10.
EP1981878B1 Indazole heteroaryl derivatives The invention relates to novel indazole derivatives as cited in claim 1, which are inhibitors of CHK1, CHK2 and SGK kinases and can be used to treat cancer and other diseases.
CN1572304A Medicinal composition for treating diabetes mellitus containing ring Pro The invention discloses a pharmaceutical composition for treating diabetes wherein the medicinal composition comprises, (1) a zinc salt including a zinc positive ion and a negative ion, (2) purified Ring-form Pro, and (3) a pharmacologically accepted excipient.
CN103127157A Medicament for curing upper respiratory tract diseases of poultry and livestock and preparation method thereof The invention relates to a medicament for curing upper respiratory tract diseases of poultry and livestock. The medicament is composed of the following components: 3-7 parts of erythromycin thiocyanate, 8-12 parts of flunixin meglumine, 0.5-2 parts of chlorpheniramine maleate and 75-85 parts of excipients. The components in the medicament participate in synergistic effect, and the untoward effects and side effects are small, so the medicament can relieve clinical symptoms of the respiratory tract diseases of the poultry and the livestock as soon as possible in the curing process, has no stimulation to stomach, is not prone to be damaged by gastric acid, and can be used as the first choice medicament for curing the upper respiratory tract infectious diseases caused by gram-positive bacteria and mycoplasma due to the fact that the dosage is less and curative effects are quite good.
US20100166799 Adenoviral vectors and methods and uses related thereto The present invention relates to the fields of life sciences and medicine. Specifically, the invention relates to cancer therapies. More specifically, the present invention relates to oncolytic adenoviral vectors and cells and pharmaceutical compositions comprising said vectors. The present invention also relates to a use of said vectors in the manufacture of a medicament for treating cancer in a subject and a method of treating cancer in a subject. Furthermore, the present invention relates to methods of producing GM-CSF in a cell and increasing tumor specific immune response in a subject, as well as uses of the oncolytic adenoviral vector of the invention for producing GM-CSF in a cell and increasing tumor specific immune response in a subject.
EP1638940B1 Pyrrolidinium derivatives as ligands for the muscarinic m3 receptor Compounds of formula (I) in salt or zwitterionic form wherein, wherein R1, R2, R3, R4, R5, J, L and M have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
EP1857112A1 Anticancer composition for oral use comprising liposome containing phytosterols and prevention or treatment for cancer using the liposome A novel use is disclosed of liposomes that contain phytosterol (e.g., β-sitosterol, campesterol, stigmasterol, brassicasterol, ergosterol, and ergostadienol, and so forth). It has been newly discovered that liposomes that contain phytosterol have a cancer metastasis inhibiting activity. Cancer metastasis is inhibited by the oral administration of liposomes that contain phytosterol and these liposomes are therefore useful for the prevention and treatment of cancer.
US20130005792 Biomarkers to identify hiv-specific t-cell subsets The invention relates to expression profiles of HIV-specific T-cells and their methods of use, including but not limited to treatment of HIV, increasing T-cell function and/or survival in HIV infected subjects, monitoring HIV disease progression and classifying HIV infected subjects as controllers or chronic progressors.
CN1915376A Slim tablet for person of to thinking to reduce weight A weight losing tablet for more quickly decreasing the fat from abdomen, lumbus, thigh and buttocks is prepared from plant extracts, amino acids, vitaminoid, minerals and additives. It features use of rice vinegar powder, apple vinegar powder and HCA substance. Its preparing process is also disclosed.
WO2008028336A1 A pharmaceutical composition of scutellarein and scutellarin or baicalin having synergistical antitumor effect A pharmaceutical composition having synergistical antitumor effect which comprises scutellarein and scutellarin or baicalin. The preparation method of said pharmaceutical composition. The use of said pharmaceutical composition in manufacturing medicament.
EP2240431A1 Crystalline modifications of (1r,2r)-3-(3-dimethylamino-1-ethyl-2-methyl -propyl)-phenol The invention relates to crystalline modifications of (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol, pharmaceutical preparations containing said modifications, and the use thereof.
US20100029661 Anesthetic compositions and methods of use The invention generally relates to anesthetic compositions comprising low doses of a selective a-2 adrenergic receptor agonists in combination with anesthetic agents. The invention also relates to methods of using these compositions; in particular, the use of these compositions in humans to enhance the efficacy of a local peripheral anesthetic injection. The compositions and the methods are particularly useful in regional block anesthetic injections, and more particularly, in dental anesthetic injections.
CN102772655A Medicine for treating beriberi and preparation method thereof The invention discloses a medicine for treating beriberi and a preparation method thereof. The medicine is composed of 40-60 g of alum, 20-30 g of sodium carbonate, 20-30 g of amur corktree, 6-15 g of essence, 20-30 g of manyflower solomonseal rhizome, 10-20 g of kochia scparia and 10-25 g of indian epimeredi herb. The medicine is convenient and quick in use, small in investment and low in cost, has no pains in treatment process, and is a relatively ideal product for treating beriberi in daily life.
WO2011142724A1 Novel antimicrobial compounds and uses thereof The present invention relates to novel antimicrobial compounds, methods of their production as well as uses thereof.
EP2051731A1 Methods for reducing the incidence of mastitis The invention encompasses methods of reducing the incidence of mastitis in an animal, and compositions and devices therefor. The methods and other aspects of the invention can be used to reduce the incidence of infection in the teat or mammary gland. In particular, but not exclusively, the invention encompasses a method of applying to the teat canal and/or teat sinus a composition comprising exogenous keratin.
WO2014145037A1 Methods and compositions for enhancing oxygen levels in tissues The present invention includes methods and compositions to enhance, inter alia, wound repair by administration of 2,3-biphosphoglycerate, myo-inositol trispyrophosphate, or a functional variant thereof.
US7605261 Urea derivatives, method for preparing same, use thereof as medicines, pharmaceutical compositions and novel use The invention relates to new products of formula (I): in which: Y represents oxygen or sulphur, Z represents C═CH2, CH—CH3 or CH2, R1 represents hydrogen, morpholinyl or the radical. In which the two nitrogen atoms are linear or form a cyclic radical, X represents carbonyl, alkylene or alkenylene, linear or branched, containing at most 6 carbon atoms optionally interrupted by oxygen or sulphur, R4, R5 and R6 represent hydrogen, a protective group of the nitrogen, alkyl, cycloalkyl, aryl and arylalkyl optionally substituted, R2 represents alkyl optionally substituted by aryl, heteroaryl or —NR4R5, R3 represents alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl optionally substituted, these products being in all isomer forms and the salts, as medicaments.
US7704971 Uracil reductase inactivators Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 alkynyl.
CN100999492A Quinoline kind iriyellowsin electronic isostericmer its preparation process and use A quinolines tectorigenin isostere, it has the right formula structure, which : R1 and R3 = Br, R2 = OR and R5=R, R4 = NO2, NR2, F, Cl, Br, OCH3 or OBn; R1 and R3 = Cl, R2 = H and R5= R, R4 = NO2, NR2, F, Cl, Br, OCH3 or OBn; R1 and R3 = F, R2 = H and R5=R, R4 = NO2, NR2, F, Cl, Br, OCH3 or OBn; R1 and R3 = H, R2=OR and R4 = OR, R5 = NO2, NR2, F, Cl or Br; the R = H, CH3 or C2H5. Experiments proved that quinolines tectorigenin isostere can inhibit the S180, EAC and HepA cells, and can inhibit five types of people cancer cells. Its activity is higher than tectorigenin itself and quinolines ketone tectorigenin isostere, so they can be used to prepare the anti-tumor drugs.
CN103275236A Preparation method of gorgon fruit polysaccharide extractive, and application thereof The invention discloses an application of gorgon fruit polysaccharide extractive in preparation of anti-fatigue drugs. According to the invention, gorgon fruit polysaccharide is extracted by a Sevag method and purified by a trichloroacetic acid method, then a pharmacological experiment is carried out by using mice as experimental subjects, and by data statistic analysis, the effects of gorgon fruit polysaccharide extractive in anti-fatigue are proved, so the invention provides theoretical basis for application of the gorgon fruit polysaccharide extractive in preparation of anti-fatigue drugs.
EP2144893A2 Tricyclic compounds as matrix metalloproteinase inhibitors The present teachings relate to compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, R4, X, and Y are as defined herein. The present teachings also provide methods of making the compounds of formula I and methods of inhibiting matrix metalloproteinases, in particular, MMP-12, that may be involved in pathological disorders found in mammals, including a human.
EP1267882B1 Prostaglandins for the treatment of eye disease caused by light irradiation like photoretinitis Disclosed is a new use of 15-keto-prostaglandin compound as an apoptosis inhibitor. Said compound can inhibit apoptosis effectively and is useful for treatment of a subject such as a human having a disease or condition associated with apoptosis.
CN101297977A Biological adhesive agent and use thereof The invention discloses a biological adhesive which is characterized in that the adhesive comprises two parts which are solute and solvent; the solute is an azide benzoylate acidylated biomacromolecule compound; the solvent can be water, water for injection, normal saline, washing liquor of Ringer solution, washing liquor of mannitol, washing liquor of dextrose, washing liquor of chlorhexidine, washing liquor of gentamicin normal saline, washing liquor of glycin, washing liquor of metronidazole or physiologic balance solution; the weight percentage concentration of the azide benzoylate acidylated biomacromolecule compound in the biological adhesive is 0.1 percent to 20 percent. When in use, the biological adhesive needs to be solidified by using ultraviolet irradiation. The biological adhesive of the invention can be used for bonding active physiological tissues, wadding and patching physiological channels, sealing surface of wound to stanch bleeding, bonding physiological materials with non-physiological materials as well as bonding non-physiological materials, with short clotting time.
US20080146509 delivery agent, parathyroid hormone, and calcitonin. This composition exhibits increased delivery of parathyroid hormone and/or calcitonin and is useful for the treatment of osteoporosis. The composition also permits simultaneous oral delivery of parathyroid hormone and calcitonin The present invention relates to a composition comprising a delivery agent, parathyroid hormone, and calcitonin. This composition exhibits increased delivery of parathyroid hormone and/or calcitonin and is useful for the treatment of osteoporosis. The composition also permits simultaneous oral delivery of parathyroid hormone and calcitonin. The composition of the present invention may be formulated into a dosage unit form, such as an oral dosage unit form. The invention also provides a method for administering parathyroid hormone and calcitonin to an animal in need thereof by administering the composition of the present invention.
WO2012047870A3 Antimicrobial preservation of propofol emulsions The invention provides intravenous formulations of propofol in an oil-in-water emulsion, having a combination of preservatives.
EP2029558A2 Compounds and methods for modulating fxr Compounds of formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
WO2013156957A1 Compounds for the prevention or treatment of infections with viruses of the flaviviridae family The present invention relates to a compound of the following formula (I): (I), or to a pharmaceutically acceptable salt thereof, for the use thereof in the prevention or treatment of an infection with a virus of the Flaviviridae family, in particular with the Hepatitis C virus (HCV), in a patient.
WO2011161282A1 Use of rapamycin for the treatment of the cognitive deficits associated with down's syndrome The present invention relates to the use of a composition comprising an inhibitor of the protein mTOR, wherein said inhibitor is selected from among rapamycin, temsirolimus, everolimus or deforolimus. Moreover, the present invention relates to use of said inhibitors, and preferably rapamycin, for the production of a medicament for the treatment of the cognitive deficit associated with Down's syndrome.
US20100247683 Methods of identifying potential components for targeted drug delivery compositions Methods of preparing compositions for preferential distribution of active agents to injury sites are provided. The compositions may comprise a polymer with hydrophilic properties and one or more active agents, such as compounds comprising hydrophilic metal ions. Because the delivery ligand and the active agent are specifically selected so the interactions between them are mainly of an ionic nature. Methods of identifying suitable components for such compositions are also disclosed.
US20080249119 Nucleosiding a protected cytosine with a protected hexose, deprotecting to obtain gemcitabine; administering as produgs; cancers of the lungs, ovaries, pancreas and bladder; cost efficiency; simplification The invention relates to homogemcitabines of general formula (2), with the meanings for the substituents as given in claim 1, method for production thereof, use for the production of the active agent gemcitabin and the use thereof for the production of medicaments for the treatment of proliferative diseases. The invention further relates to novel intermediates, as used in the inventive method.
CN103239392A Ornidazole injection preparation and preparation method The invention discloses an ornidazole injection preparation and a preparation method. The preparation method of the ornidazole injection comprises the following steps: weighing ornidazole, a pharmaceutic adjuvant and malic acid based on a formula ratio, adding injection water, stirring, dissolving, adding active carbon for adsorption, filtering, embedding, and carrying out high temperature sterilization. The ornidazole injection preparation provided by the invention is safe and reliable, has high stability and will not generate the crystallization problem if placed for a long time. The preparation method requires a simple technology, and the prepared ornidazole injection preparation meets quality requirements of a medicinal injection.
EP1299529B1 Conserved diaphanous-related formin autoregulatory domain (dad) The Diaphanous-related formins (DRFs) constitute a subclass of FH proteins known for their ability to bind activated Rho subfamily of small GTP-binding proteins which link FH proteins to cellular signalling pathways. The present inventor has identified a new homology domain unique to the DRFs that termed the DRF-autoregulatory domain (DAD) in the extreme Cterminus. DAD is involved in intramolecular binding with the GTPase binding domain (GBD) of the DRFs. Disclosed herein are compositions and methods that can disrupt this binding, and cause changes in cells including actin polymerization and/or stabilization of actin fibers resulting in growth inhibition or cell death by apoptosis. A preferred composition is peptide or polypeptide of no more than about 130 amino acids comprising the DAD peptide having the amino acid sequence [GA]-[VA]-M-D-x-L-L-E-x-L-[KRQ]-x-[GA]-[SGA]-[AP] (wherein amino acids within a set of brackets are interchangeable and x means any amino acid). Fusion proteins comprising DAD are also disclosed as are nucleic acids and expression vectors encoding these peptides and proteins.
US6902727 Synergistic mixture of polyacrolein and isothiazolin-3-one compounds A synergistic biocidal composition comprising a mixture of 2-propenal polymer (APC) and 5-chloro-2-methyl-4-isothiazoline-3-one (CIT) and 2-methyl-4-isothiazoline-3-one (MIT).
WO2007119110A3 Process for the preparation of tamsulosin and related compounds The invention relates, in general, to the preparation of (R)(-)tamsulosin free base by reaction of (R)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide or an addition salt thereof with 1 -(2-bromoethoxy)-2-ethoxybenzene in a polar aprotic solvent in the presence of an organic base. More particularly, the invention relates to a process for preparing pure solid crystalline (R)(-)tamsulosin in its free base form as a precursor for the production of (R)(-)tamsulosin hydrochloride.
CN102964361A Application of selective alpha2A receptor stimulants to treatment of Alzheimer disease The invention relates to compounds with alpha2A receptor stimulation activity in the formula (I) or pharmaceutically acceptable salts thereof. The compounds have strong activity of stimulating alpha2A receptors in vitro and the EC5alpha is at the level of nM, wherein the EC50 of the compound with the strongest activity is 15.82+/-0.95, so that the compounds can be used as neuroprotective agents to treat the Alzheimer disease.
US20120034167 Tyrosine kinase receptor tyro3 as a therapeutic target in the treatment of cancer The present invention concerns new methods for treating cancer by using TYRO3 inhibitors and methods for identifying new molecules of interest for treating cancer.
WO2014065390A1 Method for suppressing deposition of menthol whiskers The purpose of the present invention is to provide: a method for suppressing, in an easy and highly versatile manner, the deposition of menthol whiskers, said menthol whiskers being deposited when a menthol-containing solid composition is allowed to absorb moisture not only at a low to room temperature but also at a high temperature and high humidity and then the temperature is lowered; a menthol-containing solid composition wherein the deposition of menthol whiskers is suppressed; and a method for manufacturing the same. In a process for manufacturing a menthol-containing solid composition, the deposition of menthol whiskers can be suppressed simply by allowing a definite polymer to coexist with menthol.
WO2012168161A1 Combination comprising umeclidinium and a corticosteroid The present invention is directed to the combination of a muscarinic receptor antagonist and a corticosteroid, and the use of said combination in treating diseases mediated via the M3 muscarinic acetylcholine receptor and/or the glucocorticoid receptor, such as asthma.
US20100256098 Compounds for inhibiting wip1, prodrugs and compositions thereof, and related methods The invention provides compounds useful in inhibiting the activity of a Wip1 protein in a cell as well as prodrugs thereof, related methods of use and compositions which include the aforesaid compounds and prodrugs thereof. The compounds comprise a ring structure having at least five functional groups bonded thereto, wherein each functional group is bonded to a different ring atom, and wherein the at least five functional groups comprise: (a) first (R1) and second (R3) moieties each comprising a phosphate group wherein these first and second moieties are separated by at least one ring atom; (b) first (R2) and second (R4) hydrophobic groups, wherein the first and second hydrophobic groups are separated by at least one ring atom, and wherein the first hydrophobic group is bonded to a ring atom located between the ring atoms to which the first (R1) and second (R2) moieties are bonded; and an amide or carboxylic acid (R5).
CN102166195A Hydroxytyrosol pellets and preparation method thereof The invention relates to a simple, convenient and easy preparation method of hydroxytyrosol pellets. The invention comprises a technology and preparation method which avoids the problem of difficult form and bad stability of hydroxytyrosol in prior technology and provides a novel hydroxytyrosol preparation, pellets. The invention adopts a micronization technology of crushing the embedded hydroxytyrosol powder into micro powder, the average grain diameter of the micro powder is in general less than 15um, and the micro powder is mainly distributed in the range of 5-20um, so as to improve the active principle absorptivity and the bioavailability; in addition, the invention can raise the internal dissolvability of the phloretin greatly by using water-soluble adhesive and excipient, so as to improve bioavailability of the preparation and accelerate the initial time to become effective. The invention brought in pellets technology which developed rapidly in medical field, can produce the pellet-type product with controllable release in vivo and high bioavailability so as to carry out the preparation and pave the road for hydroxytyrosol application study.
US20100227865 Oligomer-Beta Blocker Conjugates The invention provides Beta-blocker drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a different biological membrane crossing rate as compared to the biological membrane crossing rate of the Beta-blocker drug not attached to the water soluble oligomer.
WO2012173448A2 Indanone derivatives, pharmaceutically acceptable salts or optical isomers thereof, preparation method for same, and pharmaceutical compositions containing same as active ingredient for preventing or treating viral diseases The present invention relates to a novel indanone derivative, pharmaceutically acceptable salts or optical isomers thereof, a preparation method for same, and a pharmaceutical composition containing same as an active ingredient for preventing or treating viral diseases. The indanone derivatives according to the present invention not only have low cyto-toxicity, but can also demonstrate utility as pharmaceutical compositions for preventing or treating viral diseases such as: polio, viral paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-mouth disease, blistering diseases, hepatitis A, myositis, myocarditis, pancreatitis, viral diabetes, epidemic myalgia, encephalitis, flu, herpes angina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis, otitis media, and the like, since excellent antiviral activity against picornaviruses such as Coxsackie virus, enterovirus, echovirus, polio virus, rhinovirus, and the like, have been demonstrated.
WO2014043442A1 Inhibition of viral infection-triggered asthma with c-kit inhibitor The invention provides methods, compositions, and kits featuring a c-Kit kinase inhibitor for use in preventing or treating virus-induced respiratory pathology.
US20080153776 Administering to an eye an aqueous solution of alginate having a minimum of about 50% mannuronate residues based upon the total number of saccharide monomeric units; no active pharmaceutical agent The present invention includes a method of treating inflammation of the eye comprising administering to an eye of a patient suffering from inflammation of the eye, a composition comprising an aqueous solution of alginate having a minimum of about 50% mannuronate residues based upon the total number of saccharide monomeric units.
US6945247 Method of treating cardio pulmonary diseases with no group compounds Treatment of pulmonary disorders associated with hypoxemia and/or smooth muscle constriction and/or inflammation comprises administering into the lungs as a gas compound with an NO group which does not form NO2/NOx in the presence of oxygen or reactive oxygen species at body temperature. Treatment of cardiac and blood disorders, e.g., angina, myocardial infarction, heart failure, hypertension, sickle cell disease and clotting disorders, comprises administering into the lungs as a gas, a compound which reacts with cysteine in hemoglobin and/or dissolves in blood and has an NO group which is bound in said compound so that it does not form NO2/NOx in the presence of oxygen or reactive oxygen species at body temperature. Exemplary of the compound administered in each case is ethyl nitrite.
DE102009015461A1 New O-acylated hydroxycarboxylic acid-polyol compounds obtained from O-acylated hydroxycarboxylic acid- and polyol-compound, useful e.g. to treat microbial diseases, preferably bacteria, virus and/or fungi/mold spores, and as food additive O-Acylated hydroxycarboxylic acid-polyol compounds (I) and their stereoisomers with D-, L- and DL-configuration obtained from O-acylated hydroxycarboxylic acid- and polyol-compounds, are new. O-acylated hydroxycarboxylic acid-polyol compounds of formula (R2-C(=O)-O-CH(C(=O)-P1)-CH(R1)-C(=O)-OR3) (I) and their stereoisomers with D-, L- and DL-configuration obtained from O-acylated hydroxycarboxylic acid- and polyol-compounds, are new. P1 : a polyol residue containing 1-10, preferably 2-6 hydroxy groups; R1 : H or -O-CO-R2; R2 : saturated linear or branched 4-26C-alkylcarboxylic acid and/or unsaturated linear or branched 4-22C-alkylcarboxylic acid; and R3 : H, Na, K, a mono-, di- or tri-ethanolammonium residue, as lysinate or ornithinate, or methyl-, ethyl-, tert-butyl-ester, or 1-4C-alkyl, and/or CH 2CH 2OH. Independent claims are included for: (1) the preparation of (I); (2) biologically active-, cosmetic- and pharmaceutical-composition comprising (I) and optionally auxiliaries and additives; and (3) a food- and cosmetic-additive containing (I), and optionally auxiliaries and additives, preferably in the form of an emulsifier, a thickening agent, a pH value controller and/or an antimicrobial agent. - ACTIVITY : Antibacterial; Virucide; Fungicide; Antidote. - MECHANISM OF ACTION : None given.
WO2008145398A1 4-arylpyrrole substituted 2-indoline derivatives active as protein kinase inhibitors The present invention relates to certain 4-arylpyrrole substituted 2-indolinone compounds of Formula (I), which modulate the activity of protein kinases (PKs). The compounds of this invention are therefore useful in treating disorders related to dysregulated PK activity The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
US7745420 stability, high effectiveness and low toxicity; for treating pulmonary/respiratory diseases such as cystic fibrosis, asthma, chronic bronchitis, chronic obstructive lung disease, eosinophilic bronchitis The invention relates to the use of nucleotide substitutes for increasing the in vivo efficacy of nucleic acid molecules and also for inhibiting inflammation in mammals. More particularly, the present invention relates to the use of 2′6′diaminopurine (DAP) and analogs thereof per se in anti-inflammatory compositions, and also for preparing nucleic acid molecules having an increased in vivo physiological efficiency and a reduced toxicity as compared to conventional oligos. The invention is particularly useful for the preparation of antisense oligonucleotides for treating pulmonary/respiratory diseases such as cystic fibrosis, asthma, chronic bronchitis, chronic obstructive lung disease, eosinophilic bronchitis, allergies, allergic rhinitis, pulmonary fibrosis, adult respiratory distress syndrome, sinusitis, respiratory syncytial virus or other viral respiratory tract infection and cancer.
EP2424495A1 Treatment of leber's hereditary optic neuropathy and dominant optic atrophy with tocotrienol quinones The present invention relates to methods of treating Leber's hereditary optic neuropathy and dominant optic atrophy with tocotrienol quinones, including alpha-tocotrienol quinone, in order to alleviate symptoms of the disease.
DE102008010579A1 Combination product obtained from a base mixture as main components, useful for the treatment of atopic dermatitis, comprises synthetic glucocorticoid, sage extract and suitable base Combination product for topical application obtained from a base mixture as main components comprises synthetic glucocorticoid, a sage extract and a suitable base. - ACTIVITY : Dermatological. - MECHANISM OF ACTION : None given.
CN103055324A Compound of co-carried cis-platinum and adriamycin, micelle and preparation method of micelle The invention provides a compound of co-carried cis-platinum and adriamycin, micelle and a preparation method of the micelle. The compound is compounded by cis-platinum, adriamycin and a segmented copolymer, wherein the cis-platinum and the segmented copolymer are compounded through coordination; the adriamycin and the segmented copolymer are compounded through electrostatic interaction; and the segmented copolymer has the structure of formula (I) or formula (II). The compound micelle of the co-carried cis-platinum and adriamycin comprises the compound of the co-carried cis-platinum and adriamycin and an aquosity medium. The preparation of the compound micelle comprises the step of reacting the adriamycin, the cis-platinum and the segmented copolymer having the structure of formula (I) or formula (II) in the aquosity medium so as to obtain the micelle of the co-carried cis-platinum and the adriamycin. The compound micelle can stably carry the cis-platinum and the adriamycin under physiological conditions, and the release of the compound micelle has pH value sensitivity.
WO2006045799A3 Pharmaceutical compositions comprising cb1 cannabinoid receptor antagonists and potassium channel openers for the treatment of diabetes mellitus type i, obesity and related conditions Described is a novel combination therapy for diabetes mellitus type I and/or for obesity and its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, by administering a combination of at least one KATP channel opener as a first active agent and at least one CB1 cannabinoid receptor antagonist as a second active agent. The invention is further directed to such novel combination therapy wherein a dually acting compound with combined KATP channel opening and CB1 antagonistic properties is used. The invention also relates to novel pharmaceutical compositions comprising KATP channel openers and CB1 antagonists and the use of said pharmaceutical compositions in the treatment, delayed progression, delayed onset of and/or inhibition of diabetes mellitus type I, and the prophylaxis and treatment, of obesity as well as the prophylaxis, treatment, delayed onset and/or inhibition of its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, in mammals and humans. The invention is further directed to such novel pharmaceutical compositions comprising a dually acting compound with combined KATP channel opening and CB1 antagonistic properties.
US20120029085 Stabilization of quinol composition such as catecholamine drugs Compositions and methods are provided for obtaining stabilized quinol compositions, such as catecholamine drugs (e.g., epinephrine solutions), and also for obtaining stable pharmaceutical formulations that comprise a stabilized quinol composition and a second pharmacologically active component such as a local anesthetic or other active drug ingredient having a reversibly protonated amine group. Stability is achieved through the inclusion of an appropriately selected pH buffer and a thiol agent, based on redox and pH buffering principles including pKa of the buffer and of the reversibly protonated amine group.
US20080312291 Heterocyclic Gaba-b Modulators The present invention relates to novel thiazole and oxazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein X1 and X2 are selected from 0 and N or S and N and R1, R2 and Y are as defined in the description. For example, R1 may be alkyl, alkoxy, thioalkoxy or aryl, R2 may be alkoxy and Y may be a carbonylamino-linked substituent containing an aryl or heteroaryl group.
EP2178869B1 Indole compounds as an inhibitor of cellular necrosis The present invention relates to indole or indazole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole or indazole compounds as an active ingredient.
US20080058308 2-carbonylamino-4,6-dihydrothieno[2,3-c]furans such as ethyl 2-{[2-fluoro-6-(trifluoromethyl)benzoyl]amino}-4-methyl-4,6-dihydrothieno[2,3-c]furan-3-carboxylate; CB2 receptors ligands for immune and inflammatory conditions; pain; neuroprotectants The present invention relates to thiophene containing compounds of formula (I) wherein R1, R2, R3, and n are as defined in the specification, pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions.
US20060252674 Methods for pretreating a subject with extracorporeal photopheresis The present invention relates to methods for treating a subject predisposed to an autoimmune disease with extracorporeal photopheresis or an effective amount of apoptotic cells before the clinical manifestation of a symptom associated with the autoimmune disease. The present invention alsorelates to methods for treating a subject predisposed to an atopic disease with extracorporeal photopheresis or an effective amount of apoptotic cells before the clinical manitfesation of a symptom associated with the atopic disease. The present invention further relates to methods for treating a transplant donor and/or a transplant recipient, or an implant recipient with extracorporeal photopheresis or an effective amount of apoptotic cells prior to the transplant or implantation procedure.
US20130034565 MOLECULES AND METHODS OF USING SAME FOR TREATING ErbB/ErbB LIGANDS ASSOCIATED DISEASES A method of selecting a target for treatment of a hyperproliferative disease in a subject in need thereof is disclosed. The method comprising analyzing an amount and/or activity of at least one ErbB ligand in a biological sample from the subject, wherein an ErbB ligand which shows an up-regulated amount and/or activity compared to a non-hyperproliferative cell or tissue above a predetermined level is selected as a target for treatment of the hyperproliferative disease. Methods of treating hyperproliferative diseases, monoclonal antibodies and pharmaceutical compositions are also disclosed.
US20120269861 Treatment of breast cancer with iodonitrobenzamides in combination with anti-tumor agents In one aspect, the present invention provides a method of treating breast cancer that is negative for ER, PR, and HER2, comprising administering to a subject at least one iodonitrobenzamide. In another aspect, the present invention provides a method of treating breast cancer comprising administering to a subject at least one iodonitrobenzamide in combination with at least one anti-tumor agent.
US6846815 Heterocyclic imines such as 2-anilino-6-quinoxalinol, used to suppress cell proliferation, differentiation, chemotaxis and/or activation; prophylaxis of restinosis; anticarcinogenic agents This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
US20130035392 Selective inhibition of the membrane attack complex of complement and C3 convertase by low molecular weight components of the aurin tricarboxylic acid synthetic complex It pertains to selective inhibition of C3 convertase of the alternative pathway of complement as well as the previously claimed assembly of the membrane attack complex of complement by use of less than 1 kDa molecular weight forms of the aurin tricarboxylic acid synthetic complex (ATAC), and their derivatives. It further pertains to the use of these materials to treat human conditions where there is evidence of self destruction of host tissue by C3 convertase activation of the alternative complement pathway, or the membrane attack complex, or both pathways. These diseases include, but are not limited to, paroxysmal nocturnal hemoglobinemia, rheumatoid arthritis, multiple sclerosis, malaria infection, Alzheimer disease, age related macular degeneration, and atherosclerosis.
EP1990342A1 Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof The invention relates to novel pyrido[2,3-b]pyrazine derivatives of general formula (I), to their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
US6875446 Method for prophylaxis and/or treatment of thromboembolism A new oral IR formulation in solid form for a low molecular weight thrombin inhibitor having pH dependant dissolution, characterized in that the formulation comprises a filler or a combination of fillers having disintegrant properties in an amount higher than 35% w/w of the formulation.
US20110152273 Fused heteroaromatic pyrrolidinones Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.
WO2012129942A1 Chiral 3-hydroxypyrid-4-one derivative, and synthesis and use thereof Disclosed are a chiral 3-hydroxypyrid-4-one derivative and a salt thereof. The compound is acquired by reacting methyl maltol or ethyl maltol with benzyl chloride to acquire a 3-benzyl protected maltol, then by reacting compound VII with different chiral amino alcohols to acquire 3-benzyloxypyrid-4-one, and finally by performing a palladium on carbon-catalyzed hydride reduction deprotection on compound IX. The compound of the present invention is capable of having iron ion chelating bioactivity, and is applicable in preparing an anti-iron overload medicament. The structure of the compound of the present invention is represented as formula (I).
US7659402 use as pain relievers, gastrointestinal disorders; 2-Amino-3-aryl-1-[3-((hetero)aryl)piperidin-1-yl]-propan-1-one compounds This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.
US20090099210 Enantiomers of selected fused heterocyclics and uses thereof This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
CN103230410A Application of zinc gluconate tablet and six-vitamin pill in treatment of ocular ametropia The invention discloses an application of a zinc gluconate tablet and a six-vitamin pill in treatment of ocular ametropia, an application of the zinc gluconate tablet and the six-vitamin pill in treatment of farsightedness or amblyopia with the diopter of +0.5D to +0.9D, an application of the zinc gluconate tablet and the six-vitamin pill in treatment of presbyopia with the diopter of +0.75D to +2.5D, an application of the zinc gluconate tablet, the six-vitamin pill and a trinosin injection in treatment of primary myopia with the diopter of -0.5D to -1.25D, and an application of the zinc gluconate tablet, the six-vitamin pill, the trinosin injection and phacolysin eye drops in treatment of primary myopia with the diopter of higher than -1.5D. A plurality of approved medicaments are adopted for new purposes, the zinc gluconate tablet, the six-vitamin pill, the trinosin injection and the phacolysin eye drops are used for treating ametropic eyes with various different diopters, and the curative effect is remarkable.
CN1628661A Enteric-coated quick releasing formulation of tannic acid and total matrine for treating enteritis The invention discloses an enteric-coated quick releasing formulation of tannic acid and total matrine for treating enteritis, wherein tannic acid total matrine and inorganic or organic basic adjuvant are employed to prepare intestine-dissolvable quick release preparation, the preparation can increase the dissolving speed in intestine, and prevent the bad stomach reaction of nausea after releasing in stomach.
WO2008013631A2 Composition for the enterosorption and management of toxins comprising a calcium aluminosilcilate clay A composition and method for use as a preventive therapy to mitigate the effects of environmental toxins, and particularly aflatoxins in a subject. The subject may be at risk for hepatocellular carcinoma and aflatoxicosis. The composition comprising: an effective amount of an isolated low sodium, calcium aluminosilicate clay in a powder form, wherein the isolated low sodium, calcium aluminosilicate clay contains acceptable levels of dioxins and priority toxic heavy metal contamination, and is capable of preferentially binding aflatoxins in the gastrointestinal tract.
WO2010119698A1 Head-and-neck tumor proliferation inhibitor Disclosed are a novel head-and-neck tumor proliferation inhibitor, a novel head-and-neck tumor metastasis inhibitor, and a novel pharmaceutical composition for treating the head and the neck. The inhibitors and the pharmaceutical composition are characterized by utilizing an inhibitor of micro RNA of which the expression is increased in head-and-neck tumor and/or a promoter of micro RNA of which the expression is decreased in head-and-neck tumor. Preferred examples of micro RNA of which the expression is increased in head-and-neck tumor include miR-455-3p, miR-455-5p, miR-130b, miR-130b*, miR-801, miR-196a, miR-21 and miR-31. Preferred examples of micro RNA of which the expression is decreased in head-and-neck tumor include miR-133b, miR-145 and miR-375.
US20080108621 Aminopterin Dosage Forms and Methods for Inflammatory Disorders There is disclosed dosage forms and methods for treating a patient with an inflammatory disorder with a therapeutically effective amount of aminopterin, or a pharmaceutically acceptable salt thereof, that achieve efficacy without concomitant toxicity. Specifically, there is disclosed a method for treating an inflammatory disorder in a patient with uninterrupted doses of aminopterin.
CN101104018A Medicinal composition for treating stomach disease and preparation process thereof The invention relates to a Chinese and western integrated medical preparation, namely, a medicine compound for treating gastropathy and the preparation method. The preparation is prepared with the following weights of raw materials: 480-800g of sodium bicarbonate, 240-360g of rhubarb, 240-360g of Chinese gentian, 240-360g of common yladimiria root, 160-240g of rhizoma corydalis yanhusuo, 20-30g of wild mint herb, 150-240g of liquorice and 15-25g of clove. The preparation can control and kill helicobacter pylori, restraint gastric acid, reduce injury to gastric mucosa, strengthen stomach and promote digestion, characterized in low cost, reliable efficacy and reasonable process.
US8232379 Nucleic acids encoding chimeric flavivirus immunogens comprising the Japanese encephalitis virus (JEV) prM signal sequence The present invention encompasses isolated nucleic acids containing transcriptional units which encode a signal sequence of one flavivirus and an immunogenic flavivirus antigen of a second flavivirus. The invention further encompasses a nucleic acid and protein vaccine and the use of the vaccine to immunize a subject against flavivirus infection. The invention also provides antigens encoded by nucleic acids of the invention, antibodies elicited in response to the antigens and use of the antigens and/or antibodies in detecting flavivirus or diagnosing flavivirus infection.
CN103156805A Ciprofloxacin thermo-sensitive type in-situ gel composition and preparing method thereof The invention discloses ciprofloxacin thermo-sensitive type in-situ gel composition and belongs to the field of veterinary drug preparations. The thermo-sensitive type in-situ gel composition comprises, by weight volume (g/ml), 5%-10% of ciprofloxacin, 20%-26% of poloxamer 407, 0.5%-10% of poloxamer 188, 0.01%-0.04% of edetic acid, 0.009%-0.03% of bacteriostatic agent, and 0.1%-0.2% of antioxidant. Solvent of the composition is acetic acid - sodium acetate buffer solution. The invention further discloses a preparing method of the composition. The ciprofloxacin thermo-sensitive type in-situ gel composition is liquid at room temperature, jelling temperature is close to body temperature, and therefore dosing is convenient and jelling speed is high, jelling strength and adhering function are good, the dosing can be achieved with accurate positioning, and loss of drug is reduced. Furthermore, the ciprofloxacin thermo-sensitive type in-situ gel composition and the preparing method thereof have controlled-releasing and long-acting functions, dosage is low, the number of times of dosing is small, harm caused by implants normally used is avoided, and pain of patients is relieved.
WO2007123187A1 Pharmaceutical composition for conformational disease Disclosed is a pharmaceutical composition having a prophylactic or therapeutic effect on a conformational disease such as Alzheimer's disease, prion disease and amyloidosis. The pharmaceutical composition comprises, as an active ingredient, at least one cellulose ether selected from a cellulose ether having a constitutional unit represented by the general formula (1) shown below, an alkali metal salt of the cellulose ether, an aliphatic acid ester of the cellulose ether, and a mixture thereof. (1) wherein at least one of R's is selected from CH3, C2H5, CH2CH2OH, CH2CH(OH)CH3 and CH2COOM, and the others are independently represent H; and M is selected from H, Na, K and Ca.
WO2013029479A1 Mycophenolic acid derivative and preparation method and use thereof Disclosed in the present invention is a mycophenolic acid derivative shown by the following general formula (V) and the pharmaceutically acceptable salts thereof, wherein L1 is -O-R2, -QCOOR2 or -QCONR2R3, Q is C1~C10. Alkylidene or C1~C6alkenylene; L2 is -O-R1 or -O-·M+. Also provided in the present invention is a pharmaceutical composition containing the mycophenolic acid derivative and pharmaceutically acceptable salts thereof and medicinal adjuvants; the preparation method of the mycophenolic acid derivative and the pharmaceutically acceptable salts thereof; and the application of the mycophenolic acid derivative and the pharmaceutically acceptable salts thereof as immunosuppressive agents.
US20120115818 Synthesis of tetracyclines and intermediates thereto Efficient method for preparing the enone intermediate (VII) used in the synthesis of tetracyclines derivatives. In particular, the invention provides a synthesis which allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
US7163672 Comprising an alkyl-polyglycoside surfactant and a medicament for inhalation The invention relates to a pharmaceutical aerosol formulation comprising a surfactant that is an alkyl-polyglycoside of formula I, wherein DP is the average degree of polymerisation and has a value of from 1 to 4, and R is an alkyl chain or a mixture of alkyl chains having a chain length of from 6 to 22 carbon atoms; or a derivative thereof for the administration of a medicament for inhalation.
CN101062919B 4-methyl-1H-diaryl pyrromonazole derivative and medicament usage thereof The invention relates to 4-metyl group-1H-diaryl pyrazole derivant and therapy salt, preparing method and usages to cure obesity, improve memory and stop smoking with therapy compound as inhibitor of inner brain cannabine I type (CB1) receptor inhibitor.
CN1775208A Liver-tonifying formulation prepared from silymarin and its preparing method The present invention relates to a Yiganling preparation prepared by using silibinin and its preparation method. It can be made into the dosage forms of dispersing tablet, soft capsule, micropills and dripping pills. The invented preparation has the action of improving liver function and protecting liver cell membrane and can be used for curing the diseases of acute hepatitis, chronic hepatitis and organizing hepatitis.
CN102091061B Application of 1,2-diphenylethylene derivative in pharmacy The invention discloses novel application of a 1,2-diphenylethylene derivative, i.e. the 1,2-diphenylethylene derivative is used as a capsaicin receptor activated synergist. The 1,2-diphenylethylene derivative in the invention and a TRPV1 (Transient Receptor Potential Vanilloid) activator have a synergistic effect. The 1,2-diphenylethylene derivative can be used as the TRVP1 activated synergist and can be applied to the preparation of a pain-easing medicine preparation.
CN101314041A Medicine carrying system of polymer micelle and preparation method thereof The invention discloses a polymer micelle medicine carrying system and a preparation method thereof. The polymer micelle medicine carrying system comprises polymer micelles formed by salicylic acid-g-chito-oligosaccharide grafts and at least one non-water soluble drug embedded in the polymer micelles, wherein the non-water soluble drug is a drug, the solubility of which in 1000ml of water medium is equal to or less than 1g. In the invention, the polymer micelles formed by the salicylic acid-g-chito-oligosaccharide grafts are used as a medicine carrier, thereby improving the medicine carrying quantity of non-water soluble drug, and simultaneously the medicine carrying system can control and release the non-water soluble drug under the condition of in vitro leak groove; moreover, the polymer micelle medicine carrying system is simple in preparation and reasonable in process.
US20130035337 Fused bicyclic heteroaryl derivative The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. A compound having the general formula (I): wherein R1 represents a C1-C6 alkyl group, a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; R2 represents a C1-C6 alkyl group; R3 represents a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; Q represents a group represented by the formula ═CH— or a nitrogen atom; and Substituent Group a represents a halogen atom, a C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, and the like, or a pharmacologically acceptable salt thereof.
WO2007039173A1 Cyclic n-[1 ,3,4]-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals The invention relates to cyclic N-[1 ,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. What is described are compounds of the formula (I) in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
WO2008137794A1 Compounds and compositions as c-kit and pdgfr kinase inhibitors The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR and PDGFR kinases.
CN102138925A Tigecycline composition and preparation method thereof The invention relates to a tigecycline composition belonging to the field of medicament preparations, in particular to a tigecycline composition suitable for injection and a preparation method thereof. The composition provided by the invention is prepared by adding one or more selected from Vitamin C or pharmaceutically acceptable salts thereof and amino acids. The tigecycline composition disclosed by the invention not only effectively restricts oxidative degradation, but also remarkably decreases the epimerization of tigecycline and improves the stability of the tigecycline.
WO2006098628A1 Oral dosage forms of gemcitabine derivatives The present invention relates to oral dosage forms of certain long chain saturated and monounsaturated fatty acid derivatives of 2',2'-difluorodeoxycytidine (Gemcitabine). In particular, the present invention relates to the use of the said gemcitabine derivatives or a pharmaceutical acceptable salt thereof for preparing an oral dosage form ameliorating compliance in treatment of cancer.
CN102140125A Novel fusidic acid derivative, preparation method and medical application thereof The invention provides a novel fusidic acid derivative shown in the following formula, wherein R represents basic amino acid residues such as lysines and arginines and can be of L-configuration, D-configuration or DL-configuration. The novel fusidic acid derivative shown in the formula can be used for preparing medicines for treating fusidic acid sensitized bacterial inflection.
WO2006114093A1 Pro-drugs of n-thiazol-2yl-benzamide derivatives The invention relates to compounds of the formula I wherein the variables are as defined in the claims. The compounds are pro-drugs of A2A-receptor ligands with improved aqueous solubility, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.
EP2363390A1 Derived lactam from d3 vitamin Compound represented by formula (1) or a pharmaceutically acceptable solvate thereof, usefull for treating or preventing Paget's disease of bone, hypercalcmia, osteoporosis or asthma. (1) R1 represents a C1-C6alkyl group or C7-C15 aralkyl group (the aromatic ring of which can be substituted by a C1-C8 alkyl group, C1-C6 alkoxy group, a hydroxyl group, a halogenatom or a trifluoromethyl group), R2 represents a C1-C6 alkyl group, and R3 represents a C1-C6 alkyl or alkoxy group, which can be substituted with a hydroxyl group.
US20130085171 Compounded transdermal pain management The present embodiments relate to topically delivered medication (compounded) for treatment of pain, inflammation, muscle fatigue, spasms, and/or other ailments. A transdermal cream may provide the effective topical administration of multiple medications simultaneously. The transdermal cream may include a salt load of approximately 30% or greater. The transdermal cream may include a unique base composition such that the transdermal cream may be able to remain stable and avoid degradation for six months or more and capable of effective delivery of active ingredient concentrations exceeding approximately 40% or more of the total formulation weight. The active ingredients may include a nerve depressant, NSAID, muscle relaxant, opiate agonist, local anesthetic, NMDA receptor antagonist, and a tricyclic antidepressant. In one embodiment, the transdermal cream may comprise ketamine HCL, gabapentin, clonidine HCL and baclofen. The transdermal cream may deliver an enhanced topical delivery flux of ketamine via a single transdermal application.
US20090181920 Intrathecal treatment of neuropathic pain with a2ar agonists The present invention relates to a method of treating neuropathic pain via intrathecal administration of agonists of A2A adenosine receptors (ARs).
US7101568 Biodegradation organophosphorus polymer; administering to tumor in situ A biodegradable polymer composition comprising: (a) a poly(phosphoester) biodegradable polymer and (b) at least one antineoplastic agent in an amount effective to inhibit the growth of a solid tumor, which is suitable for intratumoral administration to treat a mammal having a solid tumor.
CN101138560B Nitrofuran gelling agent and method of preparing the same The present invention discloses a furacilin gel and a preparation method. The weight percentages of the active component of furacilin and other components accepted for drug application comprises 0.01 percentage to 1 percentage of furacilin and 99 percentage to 99.99 percentage of the other components. The shape of the present invention is the transparent and translucent semisolid preparation. Compared with furacilin solution and ointment, the present invention has the characteristics of convenient application, cleanness and healthy property, good absorption in the skin, stability and uniform property and delight formulation.
WO2007065663A1 Quinazolinone derivatives as vanilloid antagonists The invention relates to quinazolinone compounds of the formula (I) wherein the R groups are defined in the specification, processes for their preparation and their use as pharmaceuticals, particularly in the treatment of disorders ameliorated by administration of TRPV1 antagonists.
WO2011023146A1 Imatinib mesylate polymorphs generated by crystallization in aqueous inorganic salt solutions The solution relates to a method of preparation of an imatinib mesylate polymorph as an AP1 form suitable for dosage forms. Formation of new polymorphs of tyrosine kinase inhibitors proceeds depending on the conditions, said method consisting of the following steps: a) preparation of imatinib mesylate by reaction of the imalinib base and methanesulfonic acid in aqueous environment or in a water-organic solvent mixture, with optional addition of an organic solvent; b) addition of an inorganic salt in an aqueous solution, controlling the pH and ionic strength of the solution; c) crystallization process at controlled temperature. The solution also relates to the crystalline form of imatinib mesylate polymorph and use thereof. Two new polymorphous forms of Imatinib mesylate are accessible through this method, these forms are named polymorph "Z1" and "Z2". "Z1 " is characterized by peaks in the XRPD at 5,3; 7,5; 10,0; 10,6; 14,1; 15,0 and 16;6°. "Z2" is characterized by peaks in the XRPD at 5,5; 10,6; 10,9; 14.9; 17,0 and 21,9°.
US20120270846 Preparation of an acetyl salicylic acid/glutamic acid complex for oral administration The present invention refers to a pharmaceutical preparation comprising an ionic type complex of acetyl salicylic acid and L-glutamic acid for use in the prevention or reduction of side-effects on stomach tissue associated with an oral administration of acetyl salicylic acid.
WO2005094795A1 Use of beta2-sympathomimetics for balbuties treatment Balbuties cause is avoided or reduced due to the use of the pharmaceutical products based on the selective agonists of beta-2 adrenergic receptors - β2 sympathomimetic releasing bronchoconstriction.
WO2009083521A2 Antibacterial compositions comprising an antiseptic in combination with an antibiotic The present invention relates to novel antibacterial compositions comprising particular antibiotics and antiseptics in synergic combination. These novel compositions in particular find use as a therapeutic preparation in veterinary fields contributing to environmental clean-up.
US6849642 Bicyclic imidazo-3-yl-amine derivatives substituted on the 6-membered ring Bicyclic imidazo-3-yl-amine derivatives substituted on the 6-membered ring, and pharmaceutical compositions containing these compounds, useful, inter alia, as analgesics.
WO2009111998A2 Specific impurities of montelukast The subject-matter of the invention consists in a method of removing specific impurities of montelukast of formula (I), which occur due to chemical instability of the target substance and also contaminate the substance in the preparation process. Further, methods of isolation of specific impurities of montelukast defined by formulae (V-A), (IV-A), (XIIIa-A), (XIIIb-A) and analytic methods used for the control of the production of montelukast in the pharmaceutical quality.
US20100267803 Regulators Of Fat Metabolism As Anti-Cancer Targets Embodiments of the invention provide methods of identifying agents that reduce or prevent the proliferation of breast cancer cells, or kill them, in particular by interfering with the expression of the transcription factors NR1D1 and PPARγ or the expression of genes whose transcription they activate or the activity of the proteins translated from those transcripts.
US20100178349 Pharmaceutical formulation for the production of rapidly disintegrating tablets Pharmaceutical formulation in the form of agglomerates comprising A) an excipient content composed of a) 60-97% by weight of sugar or sugar alcohols, b) 1-25% by weight of a disintegrant, c) 1-15% by weight of water-insoluble, film-forming polymers d) 0-15% by weight of water-soluble polymers and e) 0-15% by weight of further pharmaceutically customary excipients the total of the components a) to e) being 100% by weight, and B) at least one active ingredient.
WO2009117936A1 A pharmaceutical composition with effects of antipyretic, anti-inflammatory and analgesia and its preparation method A pharmaceutical composition with effects of antipyretic, anti-inflammatory and analgesia, its preparation method and its use. The pharmaceutical composition comprises gypsum 10-60 parts, and at least one material selected from the group consisting of Chuanxiong 5-15 parts and/or Angelica 5-25 parts by weight. If desired, several additional Chinese medicinal materials can be added into the composition said above, which is then prepared into any of the commonly used oral dosage forms.
CN102757338A Fenofibric urethan, preparation method and application thereof The invention relates to the technical field of medicines, particularly discloses fenofibric urethan, and meanwhile relates to a preparation method and application of fenofibric urethan. The fenofibric urethan is prepared by the reaction between fenofibric acid and urethan. The preparation method comprises the steps of adding fenofibric acid and urethan into a solvent, then reacting at room temperature until white precipitate is dissolved out, then heating to 45 DEG C-60 DEG C, keeping the temperature and reacting for 15-30min, dropwise adding diethyl ether into a reaction system until the reaction system is clear, then cooling to the room temperature, continuously reacting for 50-100min, filtering, washing a filter cake with diethyl ether, and drying to obtain fenofibric urethan. The fenofibric urethan provided by the invention can be used for effectively treating hyperlipidemia, fatty liver, hyperlipidemia and hyperglycemia disease and is good in water solubility, high in bioavailability and small in side effect.
WO2013171756A1 Amorphous form of linagliptin and process for preparation thereof The present invention relates to an amorphous form of linagliptin and processes for the preparation thereof. The invention also relates to a pharmaceutical composition comprising therapeutically effective amount of an amorphous form of linagliptin and use of said composition for treatment of diabetes especially type-I or type-II, prediabetes or reduction of glucose tolerance.
US20110020243 Methods and compositions for imaging cancer cells Disclosed are compositions comprising nanoparticles and uses thereof. Such nanoparticles include gold nanoparticles conjugated to glucose or a glucose derivative, which are useful as contrast agents in imaging methods such as computed tomography (CT). Nanoparticles disclosed herein are useful in imaging various cells, tissues, and organs, and are particularly useful in imaging tumors and tumor cells in vitro and in vivo.
US8104482 Method for treating a thrombosis A method for treating or preventing a thrombosis in a person in need thereof comprising disposing in or on an article an effective antithrombotic amount of a composition and providing the article to be in close proximity to the skin of the person, the composition comprising (i) alumina, (ii) at least one substance selected from the group consisting of silica and titanium oxide and (iii) at least one element or compound selected from the group consisting of platinum, a platinum compound, palladium, a palladium compound, iridium, an iridium compound, rhodium and a rhodium compound.
EP2103213A1 Antibacterial agent and bactericidal agent An antimicrobial agent comprising, as an active component, compounds represented by the following formula (I): [wherein, R1 and R2 each independently represent H or an alkali metal atom.]; and a microbicidal agent comprising, as an active component, compounds represented by formula (I): [wherein, R1 and R2 each independently represent H or an alkali metal atom.], wherein they have high safety and little impact on the environment.
WO2013091011A1 Heterocyclic urea compounds The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
CN1813774A Composition containing ganglioside and trivalent chromium and its use The present invention discloses a medicine composition containing ganglioside and trivalent chrome and its application in preparation of medicine and food for curing diabetes. Their mass portions are as follows: ganglioside 0.001-10000.0 portions and trivalent chrome 0.01X10 to the power-3-100.0 portions. Said invention uses trivalent chrome as kernel, and can obtain obvious effect for preventing and curing diabetes.
CN102366420A Application of Salvia polysaccharide in preparation of antioxidant medicaments or health products The invention discloses an application of Salvia polysaccharide in the preparation of antioxidant medicaments or health products. It is found through a lot of experiments that Salvia polysaccharide has high ORAC and remarkable oxidation resistance and can be use to effectively remove free radicals.
CN1784992A Method for producing sour soymilk contg. microo Yinlanzha konjak sugar for reducing-weight and lowering blood-fat A micron-class health-care sour milk for decreasing fat and losing weight is prepared from traditional milk, micron-particles of gingko leaf, gynostemma penta phyllum, haw and konjak, chitosan, isomaltose ketone and useful intestinal bacteria through proportional mixing, processing and fermenting. Its advantages are high effect and rich nutrients including vitamins, minerals, etc.
CN101352425A Compound osmotic pump controlled release preparation and preparation method thereof The invention provides a new osmotic pump controlled release pharmaceutical composition used for treating hyperlipoidemia and a preparation method thereof, the pharmaceutical composition has a nicotinic acids medicine such as acipimox and the other one estatina medicine such as simvastatin; wherein, the nicotinic acids medicine such as acipimox is a controlled release part, and the estatina medicine such as simvastatin is a quick release part; or both the acipimox and the simvastatin are the controlled release part. The compound osmotic pump preparation of the invention has the advantages of comprehensive action, low toxicity and side effects and convenient use.
CN103550223A Novel application of eye medicine wrapped with erythrocyte membrane The invention provides application of an eye medicine wrapped with an erythrocyte membrane in preparation of an eye preparation, and also provides the eye preparation. The preparation is in a form of biodegradable nano particles wrapped with the erythrocyte membrane. The preparation has the advantages that the shortcomings of the traditional eye drops that partial removal is quickly realized, the bioavailability is low, the eye drops are absorbed by the whole body, and the side effect is difficult to avoid, are overcome; the time of the medicine standing in eyes is obviously prolonged; the controlled-released administration of the medicine is realized. Therefore, the bioavailability of the medicine is improved, the side effect on the whole body is reduced, and a new hope is brought to clinical ophthalmology on treatment of intraocular diseases.
CN103432179A Compound mangosteen medicament and preparation process thereof The invention discloses a compound mangosteen medicament. The medicament is prepared by mixing the following raw materials in a weight ratio: 10g-60g of mangosteen and 0.5g-5g of L-aspartic acid calcium salt. The invention also provides a preparation process of the compound mangosteen medicament and the preparation process comprises the following steps of: (1) weighing mangosteen, refluxing and extracting with ethanol to prepare fluid extract; (2) preparing the fluid extract into extract powder; (3) granulating the extract powder, and uniformly mixing the granules and the L-aspartic acid calcium salt, and preparing a preparation by a conventional method. The medicament provided by the invention can be used for treating osteoarthritis, osteoporosis and osteoarthritis complicated with osteoporosis, is safe and effective, and has the characteristics of exact curative effect, small dosage, safe administration, no toxic or side effect and the like, compared with similar medicaments.
CN101204503A Composite of Panax notoginseng and rhizoma anemarphenae extractive The invention discloses a composition of drug combination and an application thereof, the combination comprises a notoginseng extract and an anemarrhena rhizome extract. The weight share ratio of the composition is 1:0.1-10, the better weight share ratio of the composition is 1: 0.2-5 and the best weight share ratio of the composition is 1:0.3-3. The main components are: a notoginseng total saponin, a anemarrhena saponin and saponin. The composition of the invention is able to be produced into the common drug preparation; the composition is applied for curing the cerebrovascular disease, the cerebral infarction and the cerebral stroke; and the composition is able to prevent the senile dementia, etc.
CA2211177C Agent for acting upon bone formation disturbances containing alkaline citrates, lactates and/or malates The invention relates to an agent for the prophylaxis and/or therapy of conditions associated with a disorder of bone formation. It contains alkali metal citrates and/or alkali metal lactates and/or alkali metal malates, optionally together with one or more active substances selected from vitamin K, calcium salts and vitamin D. The agent preferably contains potassium citrates and/or sodium citrates or potassium lactates and/or sodium lactates and serves for the prophylaxis and/or therapy of osteoclasis, in particular osteoporosis or osteomalacia.
US20100086519 Treatment of Hepatitis C Infection With Metalloporphyrins The present invention is directed to the treatment of hepatitis C infection with a metalloporphyrin. In particular, the present invention is based on the discovery that the NS5A protein plays a key role in HCV RNA replication by participating in polyprotein cleavage, interferon response and cellular signaling pathways. It has been found that metalloporphyrins, such as zinc porphyrins, induce post-translational down-regulation of HCV NS5A protein in an ubquitin-proteasome degradation pathway. That is, metalloporphyrins can be used to activate the ubiquitin-proteasomal pathway of NS5A protein catabolism. As a result, metalloporphyrins can be used to significantly suppress HCV viral replication in HCV infected cells.
WO2009040659A3 Benzenesulfonamide compounds and the use thereof The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
WO2010008976A3 Combined calcium, magnesium and vitamin d supplements The present invention relates to oral nutritional and therapeutic products which are useful for providing vitamins and minerals required for bone health. The present invention is an oral nutritional and therapeutic composition of calcium succinate, magnesium R-(+)-alpha-lipoate, and Vitamin D for use in the maintenance of bone health, the optimization of bone growth, reducing the risk of bone fracture, and the prevention and treatment of osteoporosis. The pharmaceutical products and methods of the present invention are particularly useful in building bone mass, quality, and density during growth, maintaining bone mass, quality, and density over time, reducing bone fracture risk, and treating osteoporosis in men and women.
CN1440745B Fluoxetine medicinal preparation Pharmaceutical formulations of fluoxetine or an acid addition salt thereof, suitable for manufacturing dispersible tablets by direct compression and comprising, in addition to the active ingredient, the appropriate excipients and coadjuvants, selected from among disintegrants, diluents, lubricants, anti-adherents, sweeteners, flavorings and, optionally, colorants. Said formulations are suitable for manufacturing dispersible tablets which disintegrate in less than three minutes in water at 19 DEG C - 21 DEG C, and are appropriate for treatment of depression.
EP2319873A1 Dextran for treating lung cancer Dextran for preparing medicine for anti-lung cancer, has repeated structure unit and molecular weight of 1.5-2.5 million Daltons. The dextran is extracted from land slug.
EP1940390A2 Antibacterial pyrrols Use of a compound of formula (I), as shown in the description, or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of bacterial infection or disease: wherein, in formula (I), A is -NR1-, -O- or -S R1 is selected from hydrogen, a halogen or a substituted or unsubstituted heterocyclic, alkyl, alkyloxy, alkylthio, alkylcarbonyl, alkyloxycarbonyl, alkylthiocarbonyl, alkenyl, alkenylcarbony, alkenyloxycarbonyl, alkenylthiocarbonyl, alkynyl, alkynylcarbonyl, alkynyloxcarbonyl, alkynylthiocarbonyl, aryl, benzyl, arylcarbonyl or aryloxycarbonyl group; and Y and Z are not identical and are independently selected from hydrogen, a halogen, or a substituted or unsubstituted heterocyclic, alkyl, alkyloxy, alkylthio, alkylcarbonyl, alkyloxycarbonyl, alkylthiocarbonyl, alkenyl, alkenyloxy, alkenylthio, alkenylcarbonyl, alkenyloxycarbonyl, alkenylthiocarbonyl, alkynyl, alkynyloxy, alkynylthio, alkynylcarbonyl, alkynyloxycarbonyl, alkynylthiocarbonyl, aryl, benzyl, aryloxy, arylthio, arylcarbonyl, aryloxycarbonyl or arylthiocarbonyl, a NR1R2 group wherein R1' and R2 are as defined for R1 or NR1'R2 is NH2.
WO2009066309A9 Process for preparation of omeprazole The present invention discloses a process for preparing 2- [(pyridinyl)methyl]sulfinyl-substituted benzimidazoles of Formula (I) or a pharmaceutically acceptable salt, hydrate, or solvate thereof. More particularly, the present invention relates to the process for oxidation of 2-[(pyridinyl)methyl]thio- substituted benzimidazoles of Formula (II).
US20120128777 Compositions containing lipid micro- or nanoparticles for the enhancement of the dermal action of solid particles The invention is related to compositions which can be used as dermal formulations for supporting the skin to restore normal conditions in case of e.g. irritated skin, or to support medical therapy of skin with atopic dermatitis symptoms, atopic dermatitis, psoriasis or related diseases (e.g. accompanied by distorted barrier function of the skin and microbial load). The compositions of the invention can be used for dermo-cosmetic products but also for pharmaceutical/-medical products, depending on the composition and the additional actives incorporated (cosmetic actives or drugs). The invention is based on the synergistic effect of metallic particles, in particular silver particles (such as microsilver, nanosilver) and lipid particles (lipid nanoparticles or lipid microparticles). As alternatives to silver particles, other metallic particles (e.g. zinc, copper) or nanocrystalline actives can be incorporated (e.g. replacing the anti-oxidative silver by anti-oxidative nanocrystals of plant molecules such as hesperitin). This leads to combinations of lipid particles with nanocrystals for dermal use.
EP1034301B1 Inhibition of an fgf-binding protein using ribozymes Increased expression of a secreted FGF-binding protein (FGF-BP) occurs in certain autoimmune and malignant disease conditions. It is found, for example, that tumor secretions of FGF-BP results in mobilization and activation of locally-stored FGFs that can serve as an angiogenic switch molecule. Furthermore, it has been found that in an animal model of multiple sclerosis (MS), the exacerbation of the disease is accompanied by increased FGF-BP. Using ribozymes, it is possible to cause cleavage of the FGF-BP mRNA. Hence, administration of ribozymes which cleave the FGF-BP mRNA in sufficient amounts to inhibit disease processes triggered by FGF-BP is appropriate.
WO2012115249A1 Crystal of spiroketal derivative The present invention provides a novel crystalline form of 1,1-anhydro-1-C-[5-(4-ethylphenyl)methyl-2-(hydroxyl- methyl)phenyl]-β-D-glucopyranose, which has a peak at a diffraction angle (2θ) around 4.0˚ in a powder X-ray diffraction pattern.
WO2012007978A3 Fermented soya based mixture comprising isoflavones- aglicones, equol and lunasil, process for the preparation and uses thereof in food, medical and cosmetic fields The present invention concerns a mixture comprising isoflavones-aglicones, such as daidzein, genistein and glycitein, in addition to equol and lunasin, said mixture being based on soya fermented using lactic acid bacteria isolated from food matrices and use of said mixture for protection of skin and similar and of human intestinal cells with particular reference to prevention of inflammatory state and protection of barrier functions and hair loss treatment.
CN1751693A Application of astragaloside in medicine for treating or preventing insulin resistance An application of astragalus polyose in preparing the medicines for preventing and treating the insulin resistant diseases, such as diabetes, obesity, diabetic hematangionosus, diabetic hepatism, etc, is disclosed.
CN101240274A Nucleic acid molecule SEPTIN1SR2 and application in preparing anti-leukemia medicament The invention belongs to abc warfare medicine field and relates to a nucleotide molecule and its use for preparing leukaemia medicaments. Leukaemia is a malignant tumo(u)r of hemapoietic system. At present, leukaemia can be treated by bone marrow grafting. Leukaemia brings prodigious burden and drang to patient and their family numbers. The nucleotide sequence of the invention comprises AUUCAUCGAGGAGCAAUUU, ATTCATCGAGGAGCAATTT, AAATTGCTCCTCGATGAAT or AAAUUGCUCCUCGAUGAAU. The nucleotide can halt lymphocyte abruption so the pharma-ceutical product composition comprising the nucleotide and transporting species or excipient vehicle in pharmacy can be used to be new pharma-ceutical product for treating leukaemia. The invention provides a new path and means for releasing and treating lymphocyte leukaemia.
CN101797257A Hormone preparation for sow aphrodisiac The invention relates to a hormone spray agent for sow aphrodisiac, which comprises the following components in percentage by weight: 0.001-0.006% of swine ectohormone, 0-5% of cosolvent and balance of a water solution containing 55-85% of ethanol, wherein the swine ectohormone is androst-16-ene-3 alpha-ol or androst-16-ene-3-one. The spray agent of the invention has simple manufacturing, can effectively improve the reproductive capacity of a sow, and promotes the development of livestock breeding.
CN101428003A Preparation of RGDF-fatty alcohol couplet mediated adriablastina target lipid and uses as anti-tumour agents The invention discloses preparation of RGDF-fatty alcohol conjugate medium adriacin target-sensitive liposomes and application thereof as antitumor agent. Antineoplastics is introduced into the amphipathic conjugate to obtain antitumor target-sensitive liposome drug, the liposome system can increase the concentration of the antineoplastics in the target position, reduce the toxic and side effects thereof in the non-target position, and improve the therapeutic index of the preparation.
US20120276111 Methods and compositions for treating conditions associated with angiogenesis using a vascular adhesion protein-1 (vap-1) inhibitor The invention relates generally to methods and compositions for treating conditions associated with angiogenesis, and, more specifically, the invention relates to methods and compositions for treating conditions associated with angiogenesis using vascular adhesion protein-1 (VAP-1) inhibitors. The invention also relates to methods and compositions for treating conditions associated with lymphangiogenesis using VAP-1 inhibitors.
EP0802921B1 Human pak65 A novel humain serine protein kinase, human p21-protein activated serine kinase p65 protein referred to as hPAK65, and methods for its preparation and use are provided. Nucleic acids encoding hPAK65 and methods for their use in preparing hPAK65 as well as in preparing and identifying hPAK65 analogs are provided. Methods provided for the use of hPAK65 protein and its protein fragments, such as those that retain at least one hPAK65 activity, that include screening libraries of agents for candidates that modulate hPAK65 activity. Methods are provided to identify agents that modulate the interaction of hPAK65 with rho-like p21 GTPases, particularly rac1 and CDC42Hs binding to hPAK65 and subsequent activation of hPAK65 serine protein kinase activity, that modulate hPAK65 serine protein kinase activity, and that modulate hPAK65 effect on p21 protein GTPase activity. Such modulating agents can provide novel chemotherapeutic agents for treatment of neoplasia, lymphoproliferative conditions, arthritis, inflammation, autoimmune diseases, apoptosis, and the like, that are related to hPAK65 and p21 protein signal transduction pathways.
CN103285032A Medicine composition for preventing and treating fungal disease of pet rabbit The invention provides a medicine composition for preventing and treating the fungal disease of a pet rabbit. The medicine composition is prepared from the following components in parts by mass: 3 parts of talcum powder, 2 parts of sulphur powder, 1 part of diaveridine and 0.5 part of clotrimazole. The medicine composition can be used for preventing and treating the fungal disease of the pet rabbit, and inhibiting, preventing and treating the occurrence and the infection of diseases caused by the fungus of the pet rabbit, so that the normal growth and development of the pet rabbit are ensured. Therefore, the medicine composition is suitable for the prevention and the treatment of fungal disease of the pet rabbits and other susceptible animals.
US8414913 Edible compositions for lowering cholesterol The present invention is related to improved compositions for reducing serum total and/or LDL cholesterol levels. The compositions are combinations of dietary fiber and plant sterol. The compositions are used as such or more advantageously in food products and comprise one or several fibers, preferably β-glucan, in combination with one or several plant sterols and/or stanols in their free and/or esterified forms.
US20110269806 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
US20100279960 Biotinylated hexadecasaccharides, preparation and use thereof The invention concerns novel biotinylated hexadecasaccharides of general formula (I) wherein: Biot is a biotin derivative; R, R1 and R2, represent independently of one another a C1-C6 alkoxy or and —OSO3; R3 represents a C1-C6 alkoxy or an —OSO3, or R3 constitutes a —O—CH2— bridge; Pe represents a saccharide concatenation; as well as their pharmaceutically acceptable salts, and their use as medicines.
US20090175941 Tablet-form slow-release preparation for vertigo The invention describes a pharmaceutical composition of a slow-release preparation in the form of tablets for the treatment of vertigo of any genesis. A pharmaceutical composition is described that contains cinnarizine and dimenhydrinate, wherein the release of active ingredients is slowed down. For this purpose, the pharmaceutical composition additionally contains binding agent, slow-release agent and fillers.
US20090082401 Deuterium-enriched tiagabine The present application describes deuterium-enriched tiagabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN102180870A (4-[2-(aryl-methyl amine)-4-methyl-thiazole-5]-pyrimidine-2)-arylamine derivative and preparation method and pharmaceutical application thereof The invention discloses a (4-[2-(aryl-methyl amine)-4-methyl-thiazole-5]-pyrimidine-2)-arylamine derivative. The structure of the derivative is shown in the specifications. The invention further provides a corresponding preparation method and finds the medical application of the derivative.
CN101317977A Nourishing beverage particle for gestation period The present invention relates to a nutritious beverage particle used in gestation. The present invention is characterized by extracting a concentrated solution from rhizoma polygonati, glossy ganoderma, dried mushroom, mulberry, heterophylly falsestarwort root, longan pulp, angelica, date, lily, reed rhizome, etc. by supercritical extraction process; preparing the concentrated solution into extract powder and evenly mixing and stirring the extract powder with folacin, VE, lysine, roxburgh rose powder, calcium gluconate and zinc gluconate; then drying, granulating and sterilizing, thus obtaining the particle.
US20090203636 Prevention and Treatment of Cancer and Other Diseases Nucleoside chemical compounds, which interact with specific structures of deoxyribonucleic acid (DNA) or ribonucleic acid (RNA) are disclosed. The compounds interfere with the activities of telomerase and reverse transcriptase, and are useful as antivirals, antibacterials and anticancer agents. Methods of treating or preventing cancers in patients involving administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases (RTs) expressed in cells of the patients are also disclosed. Method of using nucleoside analogs and other inhibitors of RTs in conjunction with DNA damaging agents such as genotoxic agents or radiation or photodynamic therapy or combinations these for the treatment of various cancers are also disclosed.
US8084441 Cystitis treatment with high dose chondroitin sulfate Interstitial cystitis and related GAG-deficient conditions of the bladder and urinary tract are treated by instillation of high dose chondroitin sulfate, such as 400 mg/20 mL. The higher dose of chondroitin is effective for the rapid reduction of symptoms, particularly in patients with severe and otherwise recalcitrant cystitis.
EP1870412A1 2-thioethenyl carbapenem derivative 2-Ethenylthio-type carbapenem derivatives of formula (I) or pharmaceutically acceptable salts thereof are provided. The compounds according to the present invention have potent antimicrobial activity and a wide antimicrobial spectrum against pneumococci including penicillin resistant Streptococcus pneumoniae (PRSP), Haemophilus influenzae including β-lactamase-negative, ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis.
WO2010080452A2 siRNA COMPOUNDS AND METHODS OF USE THEREOF The present application relates to double stranded oligonucleotide inhibitors of target genes, pharmaceutical compositions comprising same and the use of such molecules to treat, inter alia, neurodegenerative disorders including Alzheimer's disease and Amyotrophic Lateral Sclerosis, eye diseases including glaucoma and ION, acute renal failure, hearing loss, acute respiratory distress syndrome and in preventing or treating ischemia-reperfusion injury in organ transplant patients.
EP1683786A1 Vitamin d3 lactam derivative A Compound represented by the following formula (1) or pharmaceutically acceptable solvate thereof which is useful for treating Paget's disease of bone, hypercalcemia or osteoporosis. In the formula, R1 is a C2-C10 alkyl group, or a C7-C15 aralkyl group whose aromatic ring is optionally substituted with a C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxy group, a halogen atom or a trifluoromethyl group; and R2 is a C1-C10 alkyl group, or a C7-C15 aralkyl group whose aromatic ring is optionally substituted with a C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxy group, a halogen atom or a trifluoromethyl group.
CN103720703A Action of adenosine A2A receptor specific repressor on medullary respiratory center The invention discloses an action of an adenosine A2A receptor specific repressor on medullary respiratory center. The invention provides application of the adenosine A2A receptor specific repressor in preparing products with the following functions: (a) shortening inspiration time interval of hypoglossal nerve root spontaneous rhythmical respiratory discharge; (b) prolonging respiratory cycle of the hypoglossal nerve root spontaneous rhythmical respiratory discharge; (c) reducing discharge integral amplitude of the hypoglossal nerve root spontaneous rhythmical respiratory discharge; (d) reducing spike frequency of nucleus retrofacialis medial area inspiration neuron discharge; (e) shortening bursting discharge duration period of the nucleus retrofacialis medial area inspiration neuron discharge; (f) reducing bursting discharge integral amplitude of the nucleus retrofacialis medial area inspiration neuron discharge; and (g) prolonging bursting discharge interval of the nucleus retrofacialis medial area inspiration neuron discharge. The invention provides theoretical instructions and experimental references for related treatment and prevention.
CN101265259A Novel IDO inhibitor and its usage method Compositions and methods for the treatment of malignancy and chronic viral infection are disclosed. The invention especially relates to a novel IDO inhibitors and methods of use.
CN1857593B Cough-treating preparation The present invention discloses cough-treating Keliting preparation and its preparation process, and the cough-treating Keliting preparation is developed on the basis of available cough-treating Keliting syrup. The present invention has further optimized medicine material processing and improved preparation process, so that the cough-treating Keliting preparation has high medicine component leaching degree, high bioavailability, small dosage, stable medicine property and raised curative effect.
CN103751140A Cabozantinib dispersible tablets and preparation method thereof The invention discloses cabozantinib dispersible tablets and a preparation method and application thereof. The cabozantinib dispersible tablets consist of the following components in percent by weight: 10-60 percent of cabozantinib, 10-40 percent of filler, 10-50 percent of disintegrating agent, 10-50 percent of acidifying agent, 0.1-10 percent of adhesive and 0.1-20 percent of lubricating agent and flow aids. Compared with common tablets, the dispersible tablets have the advantages that the cabozantinib dispersible tablets do not contain surfactants, are high in solubleness, dispersing property and disintegration property and can be completely disintegrated within 1 minute. The cabozantinib dispersible tablets prepared by the method are high in dissolution degree, high in bioavailability, rapid in in-vivo distribution, stable in quality, good in taste, simple and feasible in preparation method and suitable for industrial production.
CN1857283A Control released gastrodin preparation The control released gastrodin preparation can maintain effective blood drug concentration for 12 hr, and has raised curative effect and lowered side effect. The control released gastrodin preparation contains gastrodin20-50 wt%, slow releasing supplementary material 50-80 wt% and other supplementary material for the rest. The film material for controlling release is cellulose acetate, ethyl cellulose, carboxypropyl methyl cellulose, polyethylene and/or polyethylene glycol. The release controlling supplementary material is polyoxyethylene, carboxypropyl methyl cellulose, Arabic gum, etc. The present invention is used widely for treating dizziness, neuralgia, headache and other diseases.
CN102772401A Novel osteoporosis resistant use of carnosol The invention discloses a novel use of carnosol for preventing and treating osteoporosis. Osteoporosis is one of the important diseases harming human health. With the aging of population, the number of patients suffering the osteoporosis is growing increasingly, so that huge social, medical and economic burdens are brought to the whole world. Although relevant experts and scholars at home and abroad pay much attention to the prevention and treatment of the disease, no effective therapeutic drug for the disease exist yet. The invention finds that the carnosol has a remarkable osteoporosis resistant effect via an in-vivo test. The test result shows that the carnosol can inhibit the enhancement of bone turnover rate caused by de-ovary, bring less destruction to the bone, can simultaneously improve blood calcium concentration and be favorable for the deposition of the bone. The carnosol has a therapeutic effect for the osteoporosis caused by oestrogen lack with no oestrogen-induced side effects.
US20140056922 Methods for using extracellular adenosine inhibitors and adenosine receptor inhibitors to enhance immune response and inflammation A method is provided herein to increase an immune response to an antigen. The method includes administering an agent that inhibits extracellular adenosine or inhibits adenosine receptors. Also disclosed are methods to increase the efficacy of a vaccine and to increase an immune response to a tumor antigen or immune cell-mediated tumor destruction.
US20070264358 Methods and Compositions for Treating Mood Disorder The invention relates to compositions and methods for treating mood spectrum disorder. The compositions relate to novel combinations and formulations of pharmaceutical compounds for treatment of mood spectrum disorders. The methods provide for use of the compounds provided herein for the treatment of mood spectrum disorders in addition to the use of mood screens for diagnosing a patient.
EP1587834B1 Uses of il-23 mammalian cytokine; related reagents Provided are methods of treatment for skin disorders. In particular, treatment, the skin disorders are generally inflammatory skin disorders, including improper wound healing. Provided are methods of using of a cytokine molecule.
EP2233471A1 A salt of 7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy}-3,4.dihydro-2(1h)-quinolinone with 5-sulfosalicylic acid and its preparation process 7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy}-3,4-dihydro-2(1H)-quinolinone salt with 5-sulfosalicylic acid and process of preparation thereof have been disclosed. On account of advantageous physico-chemical properties this salt may be applied for the manufacturing of pharmaceuticals, especially for therapeutics useful in schizophrenia treatment.
WO2013085781A1 Spirothienopyran- piperidine derivatives as orl-1 receptor antagonists for their use in the treatment of alcohol dependence and abuse The use of ORL-1 receptor antagonists of the formula (I): for the treatment of alcohol use disorders is described.
US7456177 Heteroaryl fused azapolycyclic compounds which bind to neuronal nicotinic acetylcholine specific receptor sites, and which are useful in modulating cholinergic function, for for reducing nicotine addiction or aiding in the cessation or lessening of tobacco use in a mammal, therapy The present invention provides a compound having the structure of formula I: wherein R1 is hydrogen, (C1–C6) alkyl, unconjugated (C3–C6) alkenyl, benzyl, YC(═O)(C1–C6) alkyl or —CH2CH2—O—(C1–C4) alkyl; X is CH2 or CH2CH2; Y is (C2–C6) alkylene; Z is (CH2)m, CF2, or C(═O), where m is 0, 1 or 2; R2 and R3 are selected independently from hydrogen, halogen, —(C1–C6) alkyl optionally substituted with from 1 to 7 halogen atoms, and —O(C1–C6) alkyl optionally substituted with from 1 to 7 halogen atoms, or R2 and R3 each together with the atom to which it is connected independently form C(═O), S→O, S(═O)2, or N→O; and is a 5- to 7-membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups.
CA2275153C Pharmaceutical compositions for freeze drying A pharmaceutical composition comprising a nucleotide analogue, mannitol and a modifying additve which is sodium chloride or a polyol which is suitable for freeze drying.
US20110287034 Therapeutic and diagnostic methods relating to cancer stem cells Genes that are deregulated in cancer stem cells (e.g., melanoma stem cells) are disclosed. Methods which involve modulating (e.g., inducing, inhibiting, etc.) the activity of the cancer stem cell associated genes are used to treat individuals having melanoma. Cell surface genes that are upregulated in melanoma stem cells are targeted for the selective isolation, detection, and killing of cancer stem cells in melanoma.
US20060183886 Ligands to enhance cellular uptake of biomolecules The present invention relates to the design and synthesis of homogeneous A-L-P constructs, which contain a hepatic ligand to direct an oligomer or “payload” to a hepatocyte intracellularly via a receptor-mediated, ligand-directed pathway.
CN102204902A Antrocin (Sesquiterpene lactones)-containing pharmaceutical composition for suppressing growth of cancer cells The invention relates to a pharmaceutical composition for suppressing the growth of cancer cells. The composition comprises an effective amount of compound shown as a formula I, i.e., antrocin (Sesquiterpene lactones) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
CN101015561A Compound genticin-micronomicin injection, preparing method and use thereof The invention discloses an injection of compound micironomicin sulfate, its preparation method and application. the injection comprises (by weight part) micironomicin sulfate injection 1-20, chlorpheniramine maleate 0.1-1, and dexamethasone sodium phosphate 0.01-1. the preparation method comprises heating 50% water for injection to 40-50deg.C, dissolving each components, regulating pH to 3.5-6.5 with hydrochloric acid or sodium hydroxide, and adding water for injection to 1000. The invention has the advantages of rational formulation, reduced drugfastness, and shortened withholding period. It can enhance therapeutic effect, improve swinish immunity, increase swinish body weight; and can be used for treating mycoplasmal pneumonia of pig.
US7179839 For therapy of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1–R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1–C3-alkyl), B is CH2 or CH—(C1–C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
US20110201686 Inhibitors of ASS and Synuclein Aggregation Provided are methods of inhibiting aggregation of amyloid-beta (Aβ) or accumulation of aggregated Aβ using certain guanylhydrazone compounds. Also provided are methods of treating or preventing an amyloid-related disease in a mammal, methods of treating a subject having Alzheimer's disease, methods of treating a subject at risk for Alzheimer's disease, methods of inhibiting aggregation or accumulation of a synuclein, methods of treating a subject having a disease at least partially mediated by synuclein, methods of treating a subject at risk for a disease at least partially mediated by synuclein, and methods of inhibiting aggregation or accumulation of a protein involved in a conformational disease, using the guanylhydrazone compounds.
CN101947368A Flame-retardant body strengthening safety clothing of nano-element fiber fabric The invention discloses flame-retardant body strengthening safety clothing of nano-element fiber fabric, and belongs to the field technology of production of the safety clothing of functional textile, namely flame-retardant textile. Experiments prove that the time for a person with flame-retardant clothing to escape from a fire disaster caused by a sudden accident is increased by 10 to 15 times compared with the normal person, the heat energy released by burning is only 25 percent of that of the unburned textile so as to reduce half the loss of the fire disaster, the toxic gas released by the burning is only one third of the unburned textile so as not to produce severe dense smoke, so that the life of the person can be effectively protected. Once burn and scald occur, the working clothing can effectively show an antibacterial effect, diminish inflammation, sterilize, clear away heat and toxic material, promote blood circulation and remove blood stasis, diminish swelling and promote tissue regeneration, release various macro trace elements, enhance the immunity of human body and resist against diseases.
EP1885360A2 Inhibition of neuronal damage Materials and methods for inhibiting neuronal damage are provided herein. In particular, materials and methods for inhibiting neuronal damage associated with pathological action of extracellular ATP are provided herein.
CN102872154A Application of Houttuynoid B in helicobacter pylori resistant medicament In-vitro activity experiments show that Houttuynoid B has strong helicobacter pylori (Hp) resistant activity. The Houttuynoid B can be applied to treatment of diseases such as acute and chronic gastritis and gastric and duodenal ulcer and preparation of medicaments for treating the acute and chronic gastritis and the gastric and duodenal ulcer. The invention discloses the application of the Houttuynoid B in preparation of the Hp resistant medicaments for the first time, the skeleton type belongs to a brand-new skeleton type, the Houttuynoid B has unexpected strong inhibiting activity on the Hp, the probability of giving any revelation by other compounds does not exist, and the Houttuynoid B has predominant substantial characteristics and obviously makes a remarkable progress on prevention and treatment of Hp infection.
US8449911 Drug composition having active ingredient adhered at high concentration to spherical core Granule, fine particle or tablet of excellent leaching property, comprising a drug active ingredient in high content realized by forming a layer containing drug active ingredient on core particles through a combination of a method of dispersing and adhering an active ingredient while spraying or adding a binder with a method of spraying or adding a solution or suspension wherein an active ingredient and a binder are contained so as to effect adhesion. Further, there are provided a drug composition containing such a granule, fine particle or tablet and a process for producing the same.
US20050154018 Method for treating and preventing disorders using optically pure (+) norcisapride Methods for the prevention, treatment, or management of apnea, apnea disorders, bulimia nervosa, irritable bowel syndrome, urinary incontinence, bradycardia, bradyarrhythmia, syncope, other disorders, or symptoms thereof using (+) norcisapride, or a pharmaceutically acceptable salt thereof, substantially free of its (−) stereoisomer.
US20100190702 Compositions and Methods of Treating Neoplasia The invention features compositions and methods that are useful for the treatment of neoplasia by reducing base excision repair (BER). Such compositions are useful, for example, for enhancing the efficacy of known chemotherapeutics, such as DNA alkylating agents. In particular, the invention features agents that mimic the interaction of APC with pol-β. Such agents reduce the activity of long patch- and single nucleotide-base extension repair pathways.
EP1685832B1 Nerve regeneration promoters Nerve regeneration promoters containing compounds represented by the following general formula (1), salts thereof or prodrugs of the same: (1) wherein each symbol is as defined in the specification. The compounds represented by the general formula (1) inhibit nerve cell death and promote the formation of new nerve cells and nerve cell regeneration and also promote the repair and regeneration of nerve tissues and functions through neurite extension, because of serving as a stem cell (nerve stem cell, embryonic stem cell, bone marrow cell, etc.) proliferation/differentiation promoter, a nerve cell precursor proliferation/differentiation promoter, a neurotrophic factor activity enhancer, a neurotrophic factor-like substance or a neurodegeneration inhibitor. Furthermore, these compounds are useful in preparing cells for transplantation (nerve stem cells, nerve cell precursors, nerve cells, etc.) from a brain tissue, bone marrow, embryonic stem cells, etc. At the same time, these compounds promote the take, proliferation, differentiation and function expression of transplanted cells, which makes them useful as preventives and/or remedies for neurodegenerative diseases.
CN101270139A Common camellia flavone glycosides A with estrogen liveness, preparation method and application thereof The present invention provides camellia flavonoid glycoside A with estrogenic activity, a preparation method and applications thereof. The compound is a novel compound prepared by camellia semiserrata Chi seed oil meal, the system of which is named as kaempferol-3-O-Beta-D-glucosyl-(6.1)-2'', 4''-O-diacetyl-Alpha-L-rhamanopyranosyl-(3.1)-2'', 3'', 4''-O-triacetyl-Alpha-L-rhamnoside. The compound has obvious estrogenic activity.
CN101759710A Cephalosporin derivatives containing substitutional nitrogen heterocycle The invention belongs to the technical field of medicine, in particular relating to cephalosporin derivatives containing substitutional nitrogen heterocycle shown in general formula (I), pharmaceutically acceptable salt, easily hydrolyzed ester or isomer thereof, wherein, R1, R2, R3, R4, R5, R6, X and n are defined as specification; and the invention further relates to a preparation method of compounds, a pharmaceutical composition containing the compounds, and an application of the compounds in preparing a medicine for treating and/or preventing infectious diseases.
CN1823830A Medicine and food dual purpose nutritive product for preventing pseudomyopia and real myopia and its manufacturing method A Western medicine used as both medicine and food for preventing and treating pseudomyopia and myopia is prepared from vitamins, trace elements and mineral Ca. Its preparing process is also disclosed.
CN101375835A External-use sertaconazole nitrate suppositorium The invention provides an external nitric acid Sertaconazole suppository, which is a suppository of different specifications made by mixing the powder of ground nitric acid Sertaconazole and melt suppository base, glycerol and Polysorbate 80. The suppository has the beneficial effects that the preparation process of the suppository is simple, the eutherapeutic and low-toxic nitric acid Sertaconazole are used as the main medicaments, a greater cure effect can be achieved by using a small amount of medicament for local application, mycotic infection is inhibited, the cure effect is good, the use is convenient, etc.
US20110039849 5-substituted-2-imino-thiazolidinone compounds and their use as inhibitors of bacterial infection A method for inhibiting Gram-negative bacterial pathogenesis, a method of screening for compounds that inhibit type III secretion in Gram-negative bacteria, and compounds that inhibit type III secretion in Gram-negative bacteria.
US20070149540 Crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid acetonitrile solvate; antibacterial activity; preferentially precipitated by controlling supersaturation concentration in crystalization using acetonitrile A main object is to provide a crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid acetonitrile solvate (Compound B) which is an intermediate for producing preferentially the type III crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl-1-piperazinyl]-4-oxo-4H-[1,3]-thiazeto[3,2-a]quinoline-3-carboxylic acid (Compound A). A crystal of Compound B can be preferentially precipitated by controlling the supersaturation concentration in crystalization using acetonitrile as a solvent. Subsequently, the type III crystal of Compound A can be produced by performing desolvation of the crystal.
CN102188370A Resveratrol injection solution and intravenous injection The invention relates to the technical field of medicament, in particular relates to a resveratrol injection solution and an intravenous injection thereof, wherein the resveratrol injection solution mainly comprises resveratrol, an injection solvent and a small amount of pH conditioning agent. The resveratrol intravenous injection is prepared by evenly mixing the resveratrol injection solution and the emulsion according to the volume ratio being 1:5 to 1:250 when in use. After the resveratrol injection solution and the emulsion are mixed, the drug loading rate of the resveratrol in the intravenous injection can achieve 1.5mg/ml, and the resveratrol can not be crystallized and separated out within 18 hours. The preparation method of the resveratrol injection solution is simple and safe, the solution has good stability and is convenient to store and transport, the resveratrol intravenous injection has good stability and no toxic and side effects by taking the emulsion as a carrier solution medium. According to the invention, the problem that the resveratrol can not be prepared into the intravenous injection and applied clinically for a long term is solved.
US20110028434 Long-chain polyunsaturated fatty acids (lc-pufa) in maternal nutrition during pregnancy and lactation The present invention relates in general to maternal food compositions. In particular, the present invention relates to maternal food compositions comprising LC-PUFA and their uses. Embodiments of the present invention relate to maternal food compositions comprising a source of lipids, wherein the source of lipids includes at least one LC-PUFA in the form selected from the group consisting of phospholipids (PL), phosphotidylcholine (PC), phosphatidylethanolamine (PE), N-Acylphosphatidylethanolamine (NAPE), phosphatidylinositol (Pl), phosphatidylserine (PS) or their lyso derivatives and their uses in brain development and eye development of neonates.
WO2014107713A1 Combination of a hdm2 antagonist and a mek inhibitor for use in treating cancer Methods of causing growth inhibition of cancer cells are provided, wherein the methods comprise contacting cancer cells with an HDM2 antagonist and a MEK inhibitor. Compositions in which the HDM2 antagonist and MEK inhibitor are combined also are provided.
WO2014086478A1 Inhibitors of malt1 protease The present invention relates to compounds which are inhibitors of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALTl) and to their use in therapy, in particular in the treatment or prevention of a disease or disorder which is treatable by an inhibitor of a paracaspase. The present invention also relates to pharmaceutical compositions containing such compounds.
CN102174614A Antarctic cold-adapted microbial extracellular polysaccharide capable of improving body immunity The invention relates to an Antarctic cold-adapted microbial extracellular polysaccharide capable of improving body immunity, and belongs to the technical field of medicaments and health-care food. The cold-adapted microbial extracellular polysaccharide is prepared by culturing, fermenting, separating and purifying Antarctic cold-adapted bacteria (Pseudoaltermonas sp.) S-5, the strain collection number of which is CGMCC NO.3433. The molecular weight of the polysaccharide is 39,7046Da, and the polysaccharide consists of mannose, dextrose and galactose in a molar ratio of 4.8: 50.9: 44.3. The prepared Antarctic cold-adapted microbial extracellular polysaccharide capable of improving the body immunity can promote the proliferation of in vitro spleen lymphocytes, enhance the activity of macrophages and improve the body immunity.
US20120232094 Use of adrenergic n-phenylpiperazine antagonists, pharmaceutical compositions containing them, and methods of preparing them The present invention describes phenylpiperazinyl alpha adrenergic antagonists that corresponds to the formula (I) which selectively act on the alpha 1A/alpha 1D subtypes, where its selectivity index in comparison to alpha 1B subtype is, at minimum, 1700 for the alpha 1A subtype and 10000 for the alpha 1D subtype, being therefore useful for the treatment of the lower urinary tract symptoms, including the benign prostatic hyperplasia treatment in mammals, preferentially humans. Also described are pharmaceutical compositions containing said compounds and methods for its preparation.
US6902741 Laminates containing an active substance transdermal system The transdermal system includes a sex hormone-containing adhesive matrix, which contains inclusions of a sex hormone in a hydrophilic non-crosslinked polymer in dissolved or dispersed form. The inclusions have a concentration of 20 to 90 percent by weight of the sex hormone, which is more than 50 percent by weight amorphous. The hydrophilic non-crosslinked polymer can be polyvinylpyrrolidone, methylcellulose, ethylcellulose or hydroxyethylcellulose. The adhesive matrix can be a polyisobutylene, ethylene-vinyl-acetate copolymer or a polystyrene-butadiene block copolymer.
WO2007109230A3 Nutrient compositions for the treatment and prevention of inflammation and disorders associated therewith The present disclosure describes a novel composition for the treatment and/or prevention of neurogenic inflammation. Such composition is also useful in the treatment and/or prevention of disease states and conditions associated with neurogenic inflammation. Such disease states and conditions include, but are not limited to, migraine headache, arthritis and fibromyalgia. The composition comprises nutrient compounds in a novel combination and formulation to treat and/or prevent neurogenic inflammation and disease states and conditions associated therewith. By reducing neurogenic inflammation, the compositions of the present disclosure reduce the symptoms associated with neurogenic inflammation, such as pain and systemic inflammation in general.
WO2012101487A1 Di/tri-aza-spiro-c9-c11alkanes The invention relates to compounds of the formula I A-D-C(R1)2-B (I), in which A and B are aromatic ring systems and wherein D is selected from the groups D1 to D5 and the other substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
WO2007130589A2 Nl, n4-bis (buta-i, 3-dienyl) butane-i, 4-diamine pharmaceutical compositions and uses thereof N1,N4-bis(buta-1,3-dienyl)butane-1,4-diamine dihydrochloride (also referred to as MDL 72,527 and N,N'-di-2,3-butadienyl-1,4-butanediamine dihydrochloride), or salts or solvates thereof, its use as an antioxidant, its use in preventing and/or treating prostate cancer in male humans, and its use in reducing the concentration of reactive oxygen species in human prostate gland tissue or any other body tissue, and methods of making the compound thereof. Other methods include inhibiting acetyl polyamine oxidase in human prostate tissue or other human body tissue comprising administering a therapeutic amount of N,N'-bis(2,3-butadienyl)-1,4-butanediamine or a salt or solvate thereof to the human, and a method of determining oxidative stress in human prostate tissue or other human or animal body tissue comprising measuring a ratio of oxidized 2',7'-dichlorodihydrofluorescein diacetate fluorescence :DNA fluorescence and hydroethidine dye fluorescence ex vivo or in vivo.
US20050053578 For use as wound closure adhesives A polymerizable antimicrobial formulation for forming a wound closure adhesive comprising cyanoacrylate monomer and diiodomethyl-p-tolylsulfone; and a method for closing the approximated edges of a wound with a polymeric film that substantially inhibits the growth of microorganisms, where the polymeric film is formed by use of the polymerizable antimicrobial formulation.
US20060147514 Method for introducing antisense oligonucleotides into eucaryotic cells The present invention relates to a method for introducing one or more antisense oligonucleotides into one or more eucaryotic cells using one or more lipid formulations comprising one or more cationic lipids of Formula I and optionally at least one neutral lipid. In particular, the present invention relates to a method for introducing one or more antisense oligonucleotides into one or more eucaryotic cells using a lipid formulation comprising dimethyldioctadecylammonium bromide (DDAB) and at least one neutral lipid, especially dioleylphosphatidylethanolamine (DOPE). The invention also relates to kits for carrying out the invention, compositions for carrying out the invention, and compositions formed while carrying out the invention. Further, the present invention relates to a method for inhibiting or preventing cell growth or proliferation, and a method for inhibiting or preventing expression of one or more proteins.
EP1817034A1 M1 and/or m3 receptor antagonists in combination with other actives for treating respiratory disorders The present invention relates to formulations useful for treating respiratory disorders associated with the production of mucus glycoprotein, skin disorders, and allergic conjunctivitis while substantially reducing adverse effects associated with the administration of non-selective anti-cholinergic agents and methods of use thereof. In particular, the formulations include a selective muscarinic acetylcholdine receptor subtype M1 and/or M3 antagonist such as oxybutynin in combination with one or more pharmaceutically active agents, such as desloratidine.
US8372883 Methods of using cycloalkylmethylamines The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.
US20120149723 5-methyl-piperidine derivatives as orexin receptor antagonists for the treatment of sleep disorder This invention relates to heteroaryloxy 5-methyl substituted piperidine derivatives and their use as pharmaceuticals.
US20090098084 Parp inhibitor compounds, compositions and methods of use The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.
US20120010199 Novel pyrrolinone derivative and pharmaceutical composition comprising the same The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.
CN102716493A Copolymer containing amorphous agomelatine, and preparation method, pharmaceutical composition and application thereof The invention provides a copolymer containing amorphous agomelatine. The detection of a sample of the copolymer by Differential Scanning Calorimetry (DSC) and X-ray powder diffraction shows that the sample has stable properties. The copolymer mainly comprises agomelatine raw material, carrier and solvent. The invention also provides a preparation method of the copolymer containing amorphous agomelatine, and the method has good reproducibility. The invention further provides a pharmaceutical composition containing the copolymer containing amorphous agomelatine and an application of the copolymer containing amorphous agomelatine in preparing medicines for treating depression.
CN102464729A O-quaternary ammonium salt oligochitosan vanillina Schiff base bacteriostatic agent and preparation method thereof The invention discloses a natural bacteriostatic agent, i.e., an O-quaternary ammonium salt oligochitosan vanillina Schiff base and a preparation method thereof. The preparation method comprises the following steps of: modifying C2-NH2 on the molecular structure of oligochitosan with a strong bacteriostatic action on vanillina to synthesize an oligochitosan vanillina Schiff base; and grafting a quaternary ammonium salt into C6-OH in the structure of the oligochitosan vanillina Schiff base to synthesize the O-quaternary ammonium salt oligochitosan vanillina Schiff base. The preparation method is easy to operate, an operating environment is safe, and the antibacterial property and solubility of an obtained oligochitosan derivative are improved remarkably.
CA2214418C Water-based topical cream containing nitroglycerin; method of preparation and use thereof A stable, uniform, water-based topical cream containing nitroglycerin, a penetration enhancer, water, a thickener and an emulsifier is provided. Also provided are the method of preparing the cream and the use of the cream for treating male erectile dysfunction or female anorgasmia. The present invention also relates to treating patients suffering from microvascular diseases or from injured tissue.
US7838557 treating an allergic reaction by topically administering a therapeutically effective amount of an X-ray contrast medium comprising a triiodinated benzene moiety that is completely or partially substituted, and where contrast medium is a non-ionic or ionic monomer, a non-ionic or ionic dimer The present application is directed to the use of X-ray contrast media that act as universal antigens that are labeled herein as “pseudoantigens.” X-ray contrast media have the potential to exist in an aggregated state that is greater in increased concentrations. In this aggregated state, contrast media assume the role of multivalent antigens and can successfully compete with any other antigens involved in antibody-antigen reactions that lead to anaphylaxis. In this competition, the large quantity of contrast media serves to inhibit the adverse effects of antibody-antigen reactions without the contrast media itself creating antibodies or creating toxicity problems.
WO2009015828A1 Paliperidone derivatives A compound of formula (1) is useful as a pharmaceutical and as an intermediate in making paliperidone, wherein Y is an acid-sensitive group of the formula (A') in which X represents an oxygen atom, a sulfur atom, or an -NH- group; Z represents a C2-C7 alkylene bridge; and R represents hydrogen or a C1-C4 alkyl group.
US20110112077 Quinolizidinone m1 Receptor Positive Allosteric Modulators The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
CA2233042C Specific binding members for human transforming growth factor beta; materials and methods Specific binding members comprising human antibody antigen binding domains specific for human transforming growth factor beta (TGF.beta.) bind specifically isoforms TGF.beta.2 and TGF.beta.1 or both, preferentially compared with TGF.beta.3. Specific binding members may be isolated and utilised in the treatment of disease, particularly fibrotic disease and also immune/inflammatory diseases. Therapeutic utility is demonstrated using in vitro and in vivo models. Full sequence and binding information is provided, including epitope sequence information for a particularly advantageous specific binding member which binds the active form of TGF,82, neutralising its activity, but does not bind the latent form.
EP1732902A2 Nucleoside derivatives and therapeutic use thereof The present invention relates to nucleoside derivatives represented by general formulas (I) and (II), their synthetic methods and their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included.
CN1739505A L-ornidazole injection prepn The present invention discloses L-ornidazole injection preparation as one kind of nitroimidazole antibiotics. The L-ornidazole injection preparation contains L-ornidazole or its salt or their hydrate. L-ornidazole is named chemically as S-(+)-1-(3-chloro-2-hydroxypropyl)-2-methyl-5- nitroimidazole. The L-ornidazole injection preparation is prepared with L-ornidazole, supplementary material and injection water, and may be prepared into injection for immediately injection, concentrated solution for injection after clinical re-compounding or powder for injection through further freeze drying. Compared with similar preparations, the L-ornidazole preparation has high pharmacodynamic activity, lower toxicity and stable quality.
CN1989146A Sulfated oligosaccharide derivatives The invention relates to compounds which are polysufated oligosaccharide derivatives having activity as inhibitors of heparan sulfate-binding proteins and inhibitors of the enzyme heparanase; methods for the preparation of the compounds; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment, lowering of blood triglyceride levels and inhibition of cardiovascular disease of a mammalian subject.
DE102004027353A1 Use of tamsulosin hydrochloride for treating hemorrhoids and benign blood blisters in the anus Use of tamsulosin hydrochloride (I) for treating hemorrhoids and formation of benign blood blisters in the anus. - ACTIVITY : Vasotopic. No details of tests for vasotropic activity are given. - MECHANISM OF ACTION : None given.
EP1244454B1 Use of 2-amino-3,4-dihydro-quinazolines for producing a medicament for treating or preventing diseases caused by ischaemic conditions The invention relates to the use of 2-amino-3,4-dihydro-quinazolines of formula (I) and to their pharmaceutically compatible salts for producing a medicament for treating and preventing ischaemic conditions. R1, R2 and R3 have the meanings given in the claims.
CN101032489B Cefprozil dispersible table and the preparing method The present invention is cefprozil dispersing tablet and its preparation process. The cefprozil dispersing tablet includes cefprozil 260+/-50 weight portions, microcrystalline cellulose 30+/-5 weight portions, cross-linked polyvinyl pyrrolidone as disintegrant 15+/-2.5 weight portions, polyvinyl pyrrolidone 3 +/-0.5 weight portions, fine silica gel powder 3+/-0.5 weight portions, magnesium stearate 3+/-0.5 weight portions and corrective 0.5+/-0.02 weight portions. The cefprozil dispersing tablet of the present invention has high in vivo solubility, high bioavailability and convenient taking.
WO2009049378A1 Lactone derivatives The present invention relates to bioactive lactone derivatives of formula (I) and pharmaceutical and pesticidal compositions containing them. The present invention also relates to methods of treating bacterial, protozoan, parasitic and fungal infections or treating cellular proliferative disorders and methods of controlling pests using the lactone derivatives of formula (I).
EP1505957A1 Matrix type patch containing bronchodilators The present invention relates to a matrix type patch for the transdermal delivery of a bronchodilator which is consisted of a backing layer, a pressure-sensitive adhesive layer comprising a drug, and a release liner, wherein the said pressure-sensitive adhesive layer comprises as the drug component at least one of brochodilators selected from a group consisting of formoterol, salmeterol, tulobuterol, clenbuterol and the like; cationic polymers enhancing skin-permeability of the said drug components; solubilizing agents of the drug components; and pressure sensitive adhesives. The matrix type patch according to the present invention provides high skin permeability of the drug by using cationic polymeric absorption enhancers, sustained duration of the drug action for a prolonged time and excellent adhesion to the skin without causing irritation.
WO2006057629A1 Agent for prophylaxis and treatment of a human reproductive system disorders filomek and method for the production thereof The invention relates to the pharmaceutical industry, in particular to producing medicinal agents from reproductive tissues of sea hydrobionts and can be used in the form of a prophylaxis agent for restoring a human reproductive system and for treating hormonal deviations in a hypophysis-gonads system.
CN101623265B Production process for dexamethasone sodium phosphate bulk medicament The invention provides a production process for a dexamethasone sodium phosphate bulk medicament, which dissolves certain amount of dexamethasone sodium phosphate into proper amount of water for injection and performs spray drying to obtain the dexamethasone sodium phosphate bulk medicament. The dexamethasone sodium phosphate bulk medicament can be used for preparing medicaments for treating human or mammal diseases, and is preferably prepared into injection or eye drop.
WO2012116415A1 Novel small-molecules as therapeutics The present invention provides compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful in treating central nervous system disorders, such as anxiety disorders or depression.
EP1933839A1 Phenyl-(4-phenyl-pyrimidin-2-yl)-amines for enhancing immunotolerance The use of a phenyl-(4-phenyl-pyrimidin-2-yl)-amine for the preparation of a medicament for enhancing immunotolerance in a mammal; and uses, methods, processes and pharmaceutical combinations and compositions comprising such phenyl-(4-phenyl-pyrimidin- 2-yl)-amine.
US20080279785 Novel synthetic agonists of toll-like receptors containing CG dinucleotide modifications The invention relates to the therapeutic use of oligonucleotides as immune modulatory agents in immunotherapy applications. More particularly, the invention provides immune modulatory oligonucleotide compositions for use in methods for generating an immune response or for treating a patient in need of immune modulation. The immune modulatory oligonucleotides of the invention preferably comprise novel pyrimidines and purines.
CN102558126A 2-substituted chromone compound, as well as preparation method and application thereof The invention belongs to the field of medicaments, and relates to a 2-substituted chromone compound, as well as a preparation method and application thereof. In-vitro anti-HBV (hepatitis b virus) activity test results of the 2-substituted chromone compound prove that: the 2-substituted chromone compound has remarkable anti-HBV effect, low effective concentration and low cytotoxicity. A medicinal composition can be further prepared from the 2-substituted chromone compound to be used for treating or preventing infection of hepatitis b virus, and particularly for inhibiting replication of surface antigen and e-antigen of the hepatitis b virus. The medicinal composition provided by the invention can be given nasally, orally, transdermally, parenterally, or by venous or intramuscular injection.
US7015216 Heteroaryl-β-alanine derivatives as alpha 4 integrin inhibitors Disclosed are a series of heteroaryl-β-alanine derivatives, compositions containing them, processes for their preparation and their use in medicine.
WO2012146881A1 Anti-inflammatory composition for the intestine including maltitol The present invention relates to a composition including at least maltitol for the treatment or prevention of intestinal inflammation, gastrointestinal infections, lesions, wounds or contusions of the tissue on at least one portion of the gastrointestinal tract of humans or animals.
US20110027250 Sealants for Fetal Membrane Repair The present invention provides a method for preventing or repairing damage to a fetal membrane. In one embodiment, the method comprises contacting a fetal membrane with a composition comprising a four-armed catechol-terminated polyethylene glycol (cPEG) and a biocompatible oxidant. In one embodiment, the four-armed cPEG and the biocompatible oxidant are initially contained in separate solutions, and the solutions are mixed to form the composition just prior to or at the same time that the composition contacts the fetal membrane.
CN102525942A Atorvastatin calcium enteric-coated pellet and preparation method thereof The invention belongs to the field of pharmaceutical preparations and discloses an atorvastatin calcium enteric-coated pellet and a preparation method thereof. The enteric-coated pellet is prepared through the following preparation method which comprises the following steps of: (a) preparing a spheroid or spheroid-like blank pellet core by using an extrusion-spheronization method; (b) carrying out spray coating on the blank pellet core by using an atorvastatin-calcium-containing water-soluble coating solution to obtain a drug-containing pellet core, or, further coating an isolating substance on the drug-containing pellet core; and (c) carrying out spray coating on the drug-containing pellet core coated or not coated by the isolating substance by using an enteric polymer coating solution so as to obtain the atorvastatin calcium enteric-coated pellet. According to the preparation method of the atorvastatin calcium enteric-coated pellet, the blank pellet core with low friability, higher yield, smaller grain size and bright and clean surface can be obtained, and thus, the blank pellet core is convenient to further process. According to the atorvastatin calcium enteric-coated pellet and the preparation method thereof, the atorvastatin calcium enteric-coated pellet is prepared by coating active ingredients and a functional enteric coating on the blank pellet core and has the characteristic of controllable and stable in-vitro quality.
CN101439187A Novel coupling compound of bile acid and anti-hepatitis virus medicament and medical use thereof The invention relates to a bile acid-anti-hepatitis virus drug conjugate which is shown in the following formula, non-toxic pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition containing the compounds and a use. In the structural formula of figure (I), R represents OH (bile acid) or H (ursodeoxycholic acid), A represents amino acid, n is an integer from 1 to 3, and the structure of the amino acid is D type or L type. D represents the above structure (II).
EP1915150A1 Use of thienopyridone derivatives as ampk activators and pharmaceutical compositions containing them Use of thienopyridone derivatives of formula (I), in which B, R, R6, Y and Z are as defined in the description, and their pharmaceutically acceptable salts, for the preparation of a pharmaceutical composition useful for the treatment of diabetes, metabolic syndrome, related disorders and obesity.
US7371775 nonhydroscopic, suitable for preparation of metered dose of 7-carboxymethyloxy-3',4',5-trimethoxy flavone (mucus protecting activity for gastrointestinal tract); storage stability; methylation of 3',5,7-trihydroxy-4'-methoxy flavone-7-rutinoside, followed by acetylation and deprotection The present invention relates to 7-carboxymethyloxy-3′,4′,5-trimethoxy flavone.monohydrate which is a non hygroscopic product suitable for the preparation of metered dose of 7-carboxymethyloxy-3′,4′,5-trimethoxy flavone having protective activity for gastrointestinal tract including the colon, and a preparation method and uses thereof. 7-carboxymethyloxy-3′,4′,5-trimethoxy flavone.monohydrate of the present invention has advantages such as mucus protecting activity for gastrointestinal tract including the colon, convenience for handling and storage under ordinary humidity owing to its non-hygroscopicity, and ability to contain an active compound consistently for the formulation production of a medicine. In addition, the preparation method of 7-carboxymethyloxy-3′,4′,5-trimethoxy flavone.monohydrate of the present invention reduces long steps of total synthesis and requires mild conditions for the production of a compound because autoclave condition is not necessary for methylation in this case, and makes mass-production possible without any purification process such as recrystallization or column chromatography.
CN103751110A Telomerase sensitive nano-drug carrier particles and preparation method thereof The invention discloses telomerase sensitive nano-drug carrier particles and a preparation method thereof, wherein the nano-drug carrier particles have four-layer core-shell structures: inner cores are Raman molecular labeled gold nanorods, a thin layer of solid silica shell is wrapped outside each Raman molecular labeled gold nanorod, a layer of mesoporous silica shell is wrapped outside the silica shell, and a layer of telomerase sensitive single-strand DNA (Deoxyribonucleic Acid) is wrapped outside the mesoporous silica shell; pore passages of the mesoporous silica shell are loaded with drug molecules. The nano-drug carrier particles can realize intracellular telomerase triggered drug release, and solve the difficulity of low efficacy and great toxic and side effects in the existing treatment for cancer; meanwhile, SERS (Surface Enhanced Raman Scattering) signals are integrated on the nano-drug carrier particles to realize the precise optical tracing for the nano-drug carrier particles. The nano-drug carrier particles are high in repeatability, and good in drug release properties, wherein the preparation method is easy, and meanwhile the SERS signals are strong and easy to track.
US20070265251 Muscarinic Antagonists With Parp and Sir Modulating Activity as Cytoprotective Agents The present invention relates to generally to the cytoprotective activity of mixed muscarinic inhibition/PARP modulation and in particular to the use of dual inhibitors of M1 muscarinic receptor and poly(ADP-ribose) polymerase (PARP) as neuroprotective medicaments, particularly as medicaments for the prevention and/or treatment of neurological diseases. Particularly preferred compounds are condensed diazepinones, e.g. condensed benzodiazepinones such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine.
WO2007056046A1 P2x7 receptor antagonists and methods of use The invention is directed to compounds that are P2X7 antagonist and have the formula (I) or (II) or a pharmaceutically acceptable salt, prodrug, salt of a prodrug or a combination thereof, wherein R1, R2, and R3 are defined in the specification. The invention is also directed to a method of selectively inhibiting P2X7 activity comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of formula (III), (IV) or (V) wherein R6, R7, R8, R9, R10, and R11 are defined in the specification.
CN1732902A Vitamin contained spray The invention relates to a vitamin contained spray, wherein the medicinal liquor contains one or several kinds of vitamins, greasy medicinal liquid carrying consisting one or several synthesized or natural fatty oils. The prepared spray has good stability and atomizing property.
CN103656668A Bortezomib sustained-release preparation and preparation method thereof The invention discloses a bortezomib sustained-release preparation and a preparation method thereof, and belongs to the field of nano-materials and nano drug carriers. The preparation employs carbon quantum dot labeled chitosan as a carrier. The preparation method comprises the following steps: conducting esterification reaction on peptidylborate radicals of bortezomib and hydroxy of chitosan to obtain peptidyl borate ester, thus grafting bortezomib to chitosan nanoparticles; carrying out electrostatic adsorption on surface carboxyl groups of carbon quantum dots and amino groups on chitosan in the chitosan nanoparticles, thus loading the carbon quantum dots into the chitosan nanoparticle system and preparing chitosan nanoparticle bortezomib sustained-release preparation adsorbed with carbon quantum dots and coupled with bortezomib. Compared with the prior art, the bortezomib sustained-release preparation provided by the invention and the preparation method thereof have the characteristics of feasible process, simple operation, and good targeting and controlled release properties, and have important application values in biological sensing, biomedical functional nano-materials, especially controlled release of drug carriers or preparations.
US7279502 Such as prostate cancer, prostatitis and benign prostatic hyperplasia; ethyl endcapped hepta- and nona-tetramethylenediamines and 1,2-bis(4-(ethylamino)butylaminomethyl)cyclopropane Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.
CN102872135A Application of Houttuynoid D in drug for treating renal cancer The invention discloses application of Houttuynoid D in preparing a drug for treating renal cancer, belonging to the technical field of the new use of the drug. Houttuynoid D is found to have obvious inhibition effect on the growth of human renal cancer cell line KC through MTT (Methyl Thiazolyl Ternzolinm) anticancer activity evaluation in vitro. Therefore, Houttuynoid D can be used for preparing the anti-renal cancer drug and has excellent prospects in development and application. The use of Houttuynoid D in preparing the anti-renal cancer drug involved in the invention is disclosed for thefirst time; the framework type of Houttuynoid D is a brand new framework type; and Houttuynoid D has an unexpectedly high inhibition activity for the renal cancer cells.
US20080275091 Compositions and methods for treating nocturnal acid breakthrough and other related disorders The present invention relates to, inter alia, pharmaceutical compositions comprising an acid labile proton pump inhibitor and a buffering agent; to methods for manufacture of such compositions, and to use of such compositions in treating and preventing diseases and/or disorders.
US6903121 Treatment of tumors with acetylenes disubstituted with a phenyl or heteroaromatic group and a substituted chromanyl, thiochromanyl or tetrahydroquinolinyl group in combination with other anti-tumor agents Compounds of Formula 1 Formula 1 where the symbols have the meaning described in the specification, and particularly the compound of Formula 3 Formula 3 (tazarotene) exhibit synergistic anti-proliferative effect with human recombinant interferon in the treatment of solid tumors and leukemia, particularly breast cancer and acute myeloid leukemia.
US20100150881 Compositions and Methods for Use of Scar Tissue in Repair of Weight Bearing Surfaces Compositions and methods are provided for weight bearing surface, i.e., intervertebral disc (‘disc’), between spinous processes and articular cartilage, repair. Compositions include fibrosis inducing agents for facilitating fibrosis in or on the site in need of repair in order to form fibrotic connective tissue. In addition, methods are provided for distracting the appropriate disc space during treatment of a disc in need of repair, and in particular treatment of the disc in need of repair with a fibrosis inducing agent.
CN103054804A Water-soluble asiatic acid solid dispersion and its preparing method The invention discloses a preparation method of a water-soluble asiatic acid solid dispersion, and the water-soluble asiatic acid solid dispersion prepared by the method. The method comprises: dissolving asiatic acid in an organic solvent, then adding an asiatic acid-containing organic solution into a carrier-containing organic solution, and carrying out rotary evaporation, drying and sieving, thus obtaining the solid dispersion. The asiatic acid-polymer copolymer obtained by the method disclosed in the invention changes the crystal form of asiatic acid, that is to say, asiatic acid changes to an amorphous state in terms of crystal form. Therefore, the water-solubility of asiatic acid is enhanced, so that the solubility of asiatic acid in water is greatly increased.
WO2005068429A1 Derivatives of pyridine and quinoline The invention relates to compounds having formula I, which block the biosynthesis of phosphorylcholine by selectively blocking the choline kinase enzyme in tumour cells or in cells affected by parasitic infection and which, as a result, can be used in the treatment of tumours and parasitic diseases or diseases caused by viruses and fungi in animals including humans. The invention also relates to a method of preparing the aforementioned compounds and to some intermediates resulting from said method.
WO2011148922A1 Novel quinazoline compound Provided is a quinazoline compound represented by general formula [I] or a pharmacologically acceptable salt thereof, the compound or salt having a GPR119 receptor agonistic activity and being useful as a medicine. (In formula [I], R1 represents a hydrogen atom or a halogen atom; ring A represents a 5- or 6-membered aryl ring (the aryl ring may contain one to four heteroatoms which are selected from O, S, and N and are the same or different); RA1 and RA2 each independently represents a halogen atom, cyano, etc.; ring B represents a 6- or 7-membered aliphatic nitrogenous heterocyclic group; RB1 represents a hydrogen atom or an alkyl; RB2 represents a hydrogen atom or hydroxy; and RB3 represents hydroxy, cyano, etc.)
CN102274273B Topical Chinese patent medicine for treating nasal polyps and preparation method and application thereof The invention discloses a topical Chinese patent medicine for treating nasal polyps and a preparation method and an application thereof, belonging to the technical field of treatment of ear-nose-throat diseases. The topical Chinese patent medicine is characterized in that the medicine comprises the following medicinal materials: leech, white alum, Chinese honeylocust fruits, sal-ammoniac, dahurian angelica roots, mirabilite, Java brucea fruits and depositum urinae praeparatum. The topical Chinese patent medicine is prepared by the following steps: selecting and weighing the medicinal materials, vacuum-drying at room temperature, pulverizing, sieving with a 60-mesh sieve, pulverizing at low temperature, sieving with a 320-mesh sieve, collecting sieved matters, and packaging. Compared with the prior art, the topical Chinese patent medicine disclosed by the invention can eliminate diseases of patients and promote physical and mental health, has the advantages of convenience for administration of patients, quick action and no adverse effect, and has prominent substantive features and notable progress.
US20110160210 Control of intraocular pressure using alk5 modulation agents An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.
CN102824314A Preparation method of tebipenem pivoxil granules The invention relates to the field of chemical synthesis, and discloses a preparation method of tebipenem pivoxil granules. The preparation method comprises the following steps of: grinding the following raw materials in parts by weight: 32.44 parts of tebipenem pivoxil, 31.25 parts of microcrystalline cellulose, 183.56 parts of sucrose, 2.5 parts of aspartame and 0.25 part of red iron oxide; and mixing uniformly and feeding the mixture into a dry granulator for granulation. The method disclosed by the invention adopts four accessories with wide source and better compatibility with the primary medicine tebipenem pivoxil to prepare new granules; and the prepared granules can ensure better dissolution rate, relatively low content of impurities and polymers and the like under the condition of relatively few accessories, have good quality and can be widely applied to clinical treatment.
WO2004096225A3 Use of tyrosine kinase inhibitors for treating cerebral ischemia The present invention relates to a method for treating cerebral ischemia, comprising administering a compound capable of depleting mast cells or a compound inhibiting mast cells degranulation to a human in need of such treatment. Such compounds can be chosen from tyrosine kinase inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3. Preferred compounds are 2-(3-amino)arylamino-4-aryl-thiazoles or 4-(4-methylpiperazine-l-ylmethyl)-N-[4-methyl-3-(4-pyridine-3-yl)pyrimidine-2ylamino)phenyl]benzamide(imatinib).
CA2560642C 5-aminoalkylpyrazole derivatives as pesticidal agents The invention relates to 5-aminoalkylaminopyrazole derivatives of formula (I) or salts thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).
US20080287530 Tripolide Lactone Ring Derivatives as Immunomodulators and Anticancer Agents Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.
WO2006078986A3 Quorum sensing modulators Compounds described herein are useful in modulating bacterial quorum sensing.
US20060211735 4-Arylsulphonylpiperidine derivatives for antagonism of the 5-ht2a receptor Compounds of formula (I): are selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of adverse conditions at the central nervous system, such as sleep disorders and schizophrenia.
US20110002877 PTEN Inhibitors Treat Neutropenia-Associated Pneumonia Neutropenia-associated pneumonia is treated with a therapeutically effective amount of a small-molecule PTEN inhibitor. The method may further include detecting a resultant alleviation of the neutropenia-associated pneumonia, and/or diagnosing the neutropenia-associated pneumonia. The patient may be undergoing anti-cancer chemotherapy and/or radiotherapy, and the methods may further include the step of treating the patient with broad-spectrum antibiotic therapy or granulocyte colony-stimulating factor (G-CSF) therapy.
WO2014025761A1 Methods to treat neurodegenerative diseases The present invention is based on the discovery that motor neurons derived from patients with a neurodegenerative disease have decreased delayed rectifier potassium current and increased persistent sodium current compared to motor neurons derived from control healthy individuals. The present invention is also based on the discovery that the class of compounds known as "potassium channel openers" can be used to treat neurodegenerative diseases, including ALS, Parkinson's disease, Alzheimer's disease, epilepsy, and pain.
US20050143357 Vitamin d upregulated protein 1 (vdup-) methods and uses thereof A method for selecting a compound or a composition of matter for treatment of hyperproliferative disorders of the prostate in a mammal by administering the compound or the composition to a mammal (in vivo) or to a prostate cell culture (in vitro) and assessing the effect of the compound or the composition on the content of the transcription and/or translation product of a gene under the influence of at least one regulatory region of Vitamin D upregulated protein 1 (VDUP-1) gene and optionally assessing the effect of the compound or the composition on the content of apoptosis signalling kinase (ASK-1) and/or thioredoxin, in the prostate cells of said mammal or in the cells of the prostate cell culture. A substance for use in the treatment of hyperproliferative disorders of the prostate selected by the above method, a pharmaceutical composition comprising said substance, a method of treatment by of a hyperproliferative disorder of the prostate. A gene encoding VDUP-1 or a functional equivalent thereof for use as a medicament and a vector capable of expressing VDUP-1. A method of diagnosis of a hyperproliferative disorder of the prostate in a mammal by assessing the content of the transcription and/or translation products of at least one of the genes encoding ezrin, thioredoxin, peroxiredoxin 5, cyclin-dependent kinase 4, growth response protein CL6, defender against cell death 1, CD24, osteoactivin, vitamin D-upregulated protein 1, placental growth factor gene 1+2, Gata-4, duffy blood antigen, interferon-inducible 17-kDa membrane protein, 14-3-3 protein, CD9 antigen (p24), Ste-20 related kinase, ephrin type A receptor 5 precursor, programmed cell death factor 4 and DNA-methyltransferase 3a, in cells obtained from the prostate of said mammal. A kit for use in a method of diagnosis of a hyperproliferative disorder of the prostate in a mammal.
CN1965804A Hydrogel suppository of berberine hydrochloride and preparation process thereof The invention relates to an alcaine berberine aquagel plug and relative production, wherein it comprises alcaine berberine at 4.5-13.5%, chitose at 4.5-60%, polyvinyl pyrrolidon at 13-82%, and glutaral at 9-13.5%. And the production comprises that: (1), using 0.1mol/L acetate as solvent, to dissolve chitose; (2), using distilled water as solvent to prepare polyvinyl pyrrolidon solution; (3), mixing the polyvinyl pyrrolidon solution and chitose solution; (4), adding alcaine berberine, mixing uniformly; (5), adding glutaral, mixing and pouring into plug mould; (6), cooling and drying. The inventive plug can release alcaine berberine slowly, to improve its utilization. And the clothes contacting said plug can be washed clean easily.
US6887897 Therapy for kidney disease; complexing phosphorus with calcium glutarate ; prevent forming kidney stones Methods of controlling calcium intake and phosphate metabolism and metabolic acidosis in patients suffering from renal failure and associated hyperphosphatemia or patients predisposed to development of a hyperphosphatemic condition are provided. The method in accordance with this invention comprises administering to a patient a calcium glutarate compound. Therapeutic benefit can be realized in accordance with such method by administering the compound orally to a patient to increase available calcium and contact and bind with ingested phosphate in the patient's digestive tract, and thereby prevent its intestinal absorption.
US20090118316 Methods for Augmenting Bone The present invention relates to methods of stimulating osteoblast function with a PYK2 inhibitor in subjects with osteoporosis, bone fractures, non-unions, pseudoarthroses, periodontal disease or other disorders of bone metabolism. Optionally, the method further comprises administration of a second therapeutic bone agent. The present invention also relates to methods to identify a PYK2 inhibitor effective as a therapeutic bone agent comprising administering a test agent to an osteoblast-like cell and determining if osteoblast function is stimulated. Optionally, the identifying method further comprises contacting the test agent with PYK2 and determining if PYK2 activity is inhibited.
CN101912585A Medicament for treating myoma of uterus and preparation method thereof The invention discloses a medicament for treating myoma of uterus, which is characterized by being prepared from the following raw materials in part by weight: 1 to 20 parts of rose, 1 to 20 parts of seville orange flower, 1 to 20 parts of Chinese angelica, 1 to 20 parts of red paeony root, 1 to 20 parts of szechuan lovage rhizome, 1 to 20 parts of red tangerine peel, 1 to 20 parts of rhizome pinelliae preparata, 1 to 20 parts of honey-fried liquorice root, 1 to 20 parts of pared nutgrass galingale rhizome, 1 to 20 parts of scrophularia root, 1 to 20 parts of thunberg fritillary bulb, 1 to 20 parts of dipsacus asper, 1 to 20 parts of fructus aurantii immaturus, 1 to 20 parts of sudden smile powder, 1 to 20 parts of raw hawthorn fruit, 1 to 20 parts of oyster shell, 1 to 20 parts of spreading hedyotis herb, 1 to 20 parts of zedoary and 1 to 20 parts of over 95 percent edible ethanol. The medicament can be used for oral administration and absorbed by the spleen and stomach and can be used for external use and absorbed by skin, and can be absorbed complexly in two modes of oral administration and external use. The medicament has the advantages of addressing both the symptoms and root causes along with reasonable formula, simple compatibility and definite curative effect, and is particularly suitable for infecund patients caused by blood stasis and qi depression and phlegm-damp stagnation. The invention also provides a preparation method of the medicament.
WO2010036613A1 Novel cyclic benzimidazole derivatives useful anti-diabetic agents Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK- activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and h ypertensiion.
CA2335514C Alkyl ether analogs of chlorins having an n-substituted imide ring Compounds having generic formula (I), where R1, R2 and R3 are independently alkyl of 3 through about 10 carbon atoms; provided that, R1 and R2 together contain at least six carbon atoms. The compounds have utility in photodynamic therapy in treatment of tumors and other diseases. The invention includes a method of treatment by contacting a tumor with the compound and then exposing the tumor to light.
CN102885817A Application of 1,3-dicyclopentyl substituted Ectoin in preparing drug for treating rheumatoid arthritis The invention relates to application of 1,3-dicyclopentyl-1,2,3,6-Ectoin-4,5-diethyl diformate in preparing a drug for treating rheumatoid arthritis. The drug provided by the invention is composed of 1,3-dicyclopentyl-1,2,3,6-Ectoin-4,5-diethyl diformate and pharmaceutically acceptable accessories, wherein the content of 1,3-dicyclopentyl-1,2,3,6-Ectoin-4,5-diethyl diformate is 2-20%. The drug provided by the invention is in the form of oral preparations such as tablet, capsule and the like.
WO2013020440A1 Amide derivate, and preparation method therefor, pharmaceutical composition and use thereof Disclosed are an amide derivate represented by formula (I), and a pharmaceutically acceptable salt or solvate thereof. Also disclosed are a preparation method for the amide derivate, a pharmaceutical composition containing the amide derivate and a use of the amide derivate. The amide derivate of the present invention is an 11-β hydroxysteroid dehydrogenase type I (11βHSD1） inhibitor, and is applicable in treating a variety of diseases related to 11βHSD1 expression or activity.
WO2007116980A1 Suppressor of increase in blood glucose level [PROBLEMS] To specify a substance having a higher effect among many reported chemical substances derived from natural materials which can suppress the increase in blood glucose level, and to provide a suppressor for the increase in blood glucose level which is free from the concern of deterioration in odor or flavor and is also free from the concern of adverse side-effects. [MEANS FOR SOLVING PROBLEMS] The suppressor comprises fucoxanthin as an active ingredient. Fucoxanthin may be added to a food, a beverage, a nutritional supplement, a pet food, a sanitary product, a cosmetic or a pharmaceutical product. Fucoxanthin may be selected from one extracted/purified from a natural material, one produced by organic synthesis and one synthesized in a microorganism and may be used alone or in combination.
US20100331286 Combination therapy for treatment of bone and mineral disorders for patients with impaired renal function The field of the present invention relates to novel and improved therapies for treatment of complications associated with impaired renal function. More specifically, the present invention relates to evaluating the effects of a novel renal multivitamin on Vitamin D levels, EPO dose, inflammatory (e.g., C-reactive protein) and other biomarkers in an end stage renal disease (ESRD) population on hemodialysis (HD).
CN101580477B Dehydroabietylamine derivatives and application thereof in bactericidal and antineoplastic medicaments The invention relates to dehydroabietylamine derivatives, which are prepared by using dehydroabietylamine as a matrix, introducing different substituents to different positions of a C-ring of the dehydroabietylamine, and introducing different radicals to an amino group, and is represented by the following structural formula. The dehydroabietylamine derivatives are applied to antineoplastic and bactericidal medicaments.
CN102908333A Atorvastatin calcium self-nano-emulsified soft capsule and preparation method thereof The invention discloses atorvastatin calcium self-nano-emulsified soft capsule and a preparation method thereof, falling into pharmaceutical technical field. The soft capsule is a homogeneous transparent solution formed from emulsifier, co-emulsifier and oil phase, and can be spontaneously emulsified to form emulsion drops with diameter of about 10-30 nm under condition of room temperature and mild stirring. The soft capsule is prepared by (1) swelling gelatin in a mixed solution of glycerol, light shielding agent, antioxidant and water, heating to dissolve gelatin, stirring, standing to remove bubbles, and sieving to obtain capsule solution; (2) mixing atorvastatin calcium, emulsifier, co-emulsifier and oil phase, and stirring under heating to form a homogeneous clear content solution; and (3) preparing the capsule solution and content solution into soft capsule by using HTSYS-5 intelligent experiment soft capsule machine, drying, and performing surface treatment. The soft capsule has advantages of improved bioavailability of atorvastatin calcium, simple preparation method, easy production, and wide application prospect.
CN101347512A Macleaya cordata injection and preparation thereof The invention provides a pink plumepoppy herb injection and a preparation method thereof; the pink plumepoppy herb injection is prepared by the raw materials with the following parts by weight: 30-40 parts of pink plumepoppy herb extract, 0-30 parts of latent solvent, 0.5-5 parts of anodyne and 25-70 parts of dispersion medium; the pink plumepoppy herb extract is prepared by the following procedure: pink plumepoppy herb is percolated with sulphuric acid, the percolate is subject to alcohol precipitation and is filtered and then ethanol is recycled; the pink plumepoppy herb injection of the invention can effectively restrain the growth of Gram-positive bacteria and has stronger bacteriostatic action than berberine, and diplococcus pneumoniae, staphylococcus aureus and bacillus subtilis are sensitive to the pink plumepoppy herb injection; meanwhile, the pink plumepoppy herb injection also has the function of resisting nematodes and leptospira and can inhibit and slow the body temperature raise caused by diplococcus pneumoniae; furthermore, the pink plumepoppy herb injection has the efficacies of clearing away heat and toxic materials, resisting bacteria and diminishing inflammation; the indications are yellow and white scour of piglets; the preparation method has convenient operation, high yield, low cost and strong stability of finished products.
US20090280133 Pharmaceutical compounds as inhibitors of cell proliferation and the use thereof Disclosed are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
EP1908458A1 Volatile anaesthetic with xenon An anesthetic composition (I), in the form of a combination preparation, comprises: (A) xenon (Xe) or Xe containing gas, and (B) a volatile anesthetic (VA). An independent claim is also included for a gas mixture (II) for anesthesia, comprising Xe (10 - 65 vol.%), VA, oxygen and inert gas(es) to a total of 100 vol.%. - ACTIVITY : Inhalation anesthetic. In anesthesia tests in pigs using combinations of Xe and halothane, the minimal alveolar concentration (MAC) of halothane was 0.88 (by probit analysis) or 0.93 (by empirical measurement) in presence of 15 vol.% Xe, compared with 1.02 (by probit analysis) or 1.08 (by empirical measurement) in the absence of Xe. - MECHANISM OF ACTION : None given in the source material.
CN101416949A Pharmaceutical compositions of estrogenic agents This invention comprises novel pharmaceutical carrier or excipient systems and oral pharmaceutical formulations comprising as an active ingredient raloxifene, amoxifen, droloxifene, arzoxifene, or CP 336156, or analogs thereof, or a compound of the formulae I or II wherein Z is a moiety selected from the group of: wherein: R1 is selected from H, OH or the C1-C12 esters alkyl ethers thereof, benzyloxy, or halogen; or C1-C4 halogenated ethers; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or alkyl ethers thereof, halogens, or C1-C4 halogenated ethers, cyano, C1-C6 alkyl, or CF3, with the proviso that, when R1 is H, R2 is not OH; Y is the moiety: R7 and R8 are alkyl or concatenated together to form an optionally substituted, nitrogen-containing ring; or a pharmaceutically acceptable salt thereof; and excipients chosen from pharmaceutical fillers, glidants, lubricants, wetting agents and antioxidants.
WO2013067612A1 Pharmaceutical composition for the preparation of a drug for treating neuropathic pain, chronic degenerative disease-related pain and post-operative pain in animals The present invention relates to the development of a pharmaceutical composition characterized by comprising triancinolone, bupivacaine and ethanol in the form of a suspension, the use thereof characterized by being for the preparation of a drug for treating neuropathic pain, chronic degenerative disease-related pain and post-operative pain in small and large animals. The neurolytic suspension proposed promotes potent long-lasting neurolysis by means of perineural infiltration, without local adverse reactions, resulting in the therapeutic effect of eliminating pain, said neurolytic suspension being recommended for neuropathic pain, chronic degenerative conditions and post-operative pain in large and small animals.
WO2011133385A3 Novel ether-based compounds and their use This invention relates to compounds having the structure herein X, Y, A, B, and L are further described herein.
WO2008054639A3 Use of a catechin or polyphenol to treat ocular diseases and infection The invention provides compositions and methods of treating an ocular condition by administering to an eye of a patient having an ocular condition an effective amount of a catechin or polyphenol. The compositions and methods can be used to treat ocular conditions such as ocular infection, ocular inflammation, ocular cancer or benign eye tumors.
CN1839817A Anticancer slow release injection containing taxone Disclosed is a taxone-containing anticancer slow release injection comprising slow release microballoons and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The anticancer active constituents include taxone or taxone synergistic agent, the taxone synergistic agent is selected from antineoplastic antibiotics, antimetabolites and/or plant alkaloids, the slow release auxiliary materials are selected from the copolymer of polylactic acid, polyglycolic acid and glycolic acid, ethylene-vinyl acetate copolymer, or copolymer of aliphatic acid and sebacic acid, the suspension adjuvant is selected from sodium carboxymethylcellulose and Tween-80. The slow release microballoons can also be prepared into the form of slow release implantation agent.
EP1918286A1 Thiazolhydrazides for treatment of neurodegenerative diseases The present invention relates to compounds of formula (I) having a thiazolhydrazide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said thiazolhydrazide compounds can be used for prophylaxis and/or treatment of neurodegenerative diseases and conditions. Formula (I)
US20120058204 Use of over expression of cystathionine gamma lyase as a prognostic, diagnostic and therapeutic target for cancer The present invention relates to a method of identifying an expression level of cystathionine gamma lyase (CTH) in a sample from a subject. The present invention further discloses a method of diagnosing a subject with cancer having risk of resistance to a platinum-based drug. The present invention also discloses a method for improving efficacy of a platinum-based drug in a subject suffering a cancer.
CN103228270A A pharmaceutical combination comprising an ileal bile acid transport system (IBAT) inhibitor and a bile acid binder The present invention relates to a combination comprising a substance with inhibiting effect on the ileal bile acid transport system (IBAT) and at least one other active substance selected from an IBAT inhibitor; an enteroendocrine peptide or enhancer thereof; a dipeptidyl peptidase-IV inhibitor; a biguanidine; an incretin mimetic; a thiazolidinone; a PPAR agonist; a HMG Co-A reductase inhibitor; a bile acid binder; and a TGR5 receptor modulator; wherein the IBAT inhibitor compound and the at least one other active substance are administered simultaneously, sequentially or separately.
CN102344408A Double-effect anesthetic The invention discloses a double-effect anesthetic represented by a structural formula (I). With the anesthetic, frequencies of administration can be reduced, an anesthesia induction process is more convenient, and adverse reactions caused by single-agents can be reduced. The anesthetic provided by the invention is advantaged in fast effect, short duration, high anesthesia efficacy, high controllability during operation, and fast recovery after operation.
CN102861085A Application of Houttuynoid E in medicine for treating or preventing renal fibrosis The invention provides application of Houttuynoid E in preparation of a medicine for treating or preventing renal fibrosis, belonging to the technical field of new application of medicine. The application of the Houttuynoid E on preparation of the medicine for treating or preventing renal fibrosis provided by the invention is disclosed firstly. The skeleton type belongs to new skeleton type, and the inhibitory activity of Houttuynoid E on renal fibrosis is unexpectedly strong; and the probability that any revelation is provided by other compounds does not exist, Houttuynoid E has the excellent substantive features, and Houttuynoid E obviously has a remarkable progress when being used for treating or preventing renal fibrosis.
CN101890037A Nuezhenoside and hyperin composition and application thereof for preparing medicine The invention relates to a nuezhenoside and hyperin composition which is prepared from 20%-80% of nuezhenoside and 80%-20% of hyperin in proportion by weight. The composition can be used as a neuraminidase inhibitor for preventing and treating flu and be prepared into preparations acceptable pharmaceutically.
CN101134024A Hydrochloric acid ondansetron oral cavity disintegrating lyophilized tablets and method for preparing the same The present invention relates to an antitumor auxiliary medicine which can be quickly disintegrated in mouth cavity and can be quickly absorbed. It is characterized by using ondansetron hydrochloride as main medicine, adding proper filling agent and corrective to make them into solution, then making said solution undergo the process of freeze-drying treatment so as to obtain the invented oral disintegrant tablet.
CN102784155A Application of stilbeneglycoside to prophylaxis and treatment of osteoporosis The invention discloses application of stilbeneglycoside (TSG) to prophylaxis and treatment of osteoporosis. TSG has no toxic effect on osteoblast precursor cells, and does not affect cell proliferation; TSG has protective function on apoptosis of osteoblast precursor cells (MC3T3-E1) caused by hydrogen peroxide (H2O2), improves oxidative stress state induced by H2O2 in a differentiation process of the MC3T3-E1, and has protective function on MC3T3-E1 osteogenic differentiation inhibition caused by H2O2; besides, TSG can inhibit expression of a bone absorption factor. Therefore, TSG can play a role of protecting osteoporosis through improvement on osteoblast apoptosis and differentiation inhibition, and indirect inhibition of osteoclast activation.
WO2012176952A1 Aptamer which selectively binds to erbb2 receptor and uses thereof The present invention relates to a DNA aptamer which selectively binds to a breast cancer-related Her2 (ERBB2) receptor, and a composition for inhibiting cancer metastasis and a composition for diagnosing cancer which contain the DNA aptamer as an active ingredient, wherein the aptamer has a binding mechanism different from existing antibodies and thus can more effectively inhibit cancer metastasis and diagnose cancer.
EP2511275A1 Novel piperidinyl monocarboxylic acids as S1P1 receptor agonists The present invention relates to novel compounds acting as agonists at S1P (sphingosine-1-phosphate) receptors, compositions containing these compounds, use of these compounds in medicine and their process of preparation.
WO2013073577A1 Dihydroxy aromatic heterocyclic compound [Problem] To provide a compound which has a D-amino acid oxidase (DAAO) inhibitory effect and is useful, for example, as a prophylactic and/or therapeutic agent for schizophrenia and neuropathic pain. [Solution] The inventors have achieved the present invention by studying on compounds that inhibit DAAO and confirming that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory effect. Namely, a dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory effect and is applicable, for example, as a prophylactic and/or therapeutic agent for schizophrenia and neuropathic pain.
EP2777707A1 Method of Treating Brain Tumors Provided herein are methods useful for treating a brain tumor in a subject in need thereof, comprising administering to said subject an active agent comprising poly-FdUMP or a pharmaceutically acceptable salt thereof. Also provided are compositions comprising poly-FdUMP and one or more additional active agents useful for treating a brain tumor.
US20110009408 Methods for identifiying inhibitors against viruses that use a class i fusion protein The invention concerns the generation of a three dimensional model of the six helix bundle (6HB) complexed with an inhibitor and the use of that model to identify, screen and/or develop inhibitors against viruses that use a class I fusion protein. Such inhibitors of viruses that use a class I fusion protein may be effective for treating, for example, respiratory infections by Respiratory Syncytial Virus (RSV).
WO2012002773A3 Phenylcarbamate compound and muscle relaxant containing the same A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
US7084165 Monoamine reuptake inhibitors for treatment of CNS disorders The present invention relates to compounds that are useful exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and their pharmaceutically acceptable salts, and their use in the treatment of central nervous system and other disorders.
CN101928228A Amantadine derivative with anti-influenza virus activity and preparation method thereof The invention discloses an amantadine derivative with anti-influenza virus activity and a preparation method thereof, which relate to the field of organic medicinal chemistry. A group of N-substituted amantadine derivatives and medicinal salts thereof have the following chemical structures as shown in the specification, wherein I-1:R=H, I-2:R=CH3, I-3:R=CH(CH3)2, I-4:R=CH2CH(CH3)2, I-5:R=CH(CH3)(C2H5), and I-6:R=CH2Ph. The preparation method comprises the following steps: taking amantadine as a starting raw material, carrying out condensation reaction with Boc protected glycine, L-alanine, L-valine, L-leucine, L-isoleucine and L-phenylalanine in a non-protonic solvent in the presence of EDC/triethylamine, and removing the Boc protective groups by trifluoroacetic acid. The testing compound has an inhibiting effect on influenza A3 virus, and the effects of the derivatives I-1 and I-2 are the best.
US20080269205 Methods to prevent vertical transmission of infectious diseases The present invention presents a method of preventing vertical transmission of an infectious disease comprising: (a) applying a photosensitizing composition to host tissues of birth canal of a mother during the intrapartum period; and (b) applying light to the host tissues after the step (a) at a wavelength absorbed by the photosensitizing composition so as to inhibit or eliminate infectious disease microorganisms that come into contact with the host tissues. The infectious disease may be caused by human immunodeficiency virus type 1, hepatitis B virus, hepatitis C virus, Group B Streptococcus, cytomegalovirus, Listeria monocytogenes, Chiamydia trachomatis, Escherichia coli, herpes simplex virus, Epstein-Barr virus, Toxoplasma gondii, human papilloma virus, and Candida.
WO2014004543A1 Combination cancer therapy using bisphosphonates and anti-egfr agents The present invention relates to combination therapies for the treatment of EGFR-related diseases, particularly EGFR-related cancers. This invention also relates to a method of enhancing the efficacy of an EGFR family member antagonist and therapeutic methods for subjects who are refractory to treatment with an EGFR family member antagonist. The invention also relates to pharmaceutical compositions useful for treatment of EGFR-related diseases.
CA2324001C Retinoid-like compounds for the promotion of melanin production An in vitro assay for selecting compounds that alter pigmentation of skin is provided. Also, a novel class of pro-pigmentatory compounds is provided which comprise substituted aromatic or heterocyclic carboxylic acids, or derivatives thereof, or pharmaceutically acceptable salts, which do not contain a pheno, naphthol, thiophenol, or a thionaphthol function in free or protected form. In a preferred embodiment, thess compounds will display activity for RXRs. These compounds may be used for altering pigmentation of human skin and/or hair in cosmetic or dermatological compositions, and for the treatment of disorders and disease conditions that affect skin or hair pigmentation.
WO2010130934A2 2-cycloamino-5-(pyridin-4-yl)imidazo[2,1-b][1,3,4]thiadiazole derivatives, preparation thereof, and therapeutic use thereof The invention relates to 2-cycloamino-5-(pyridin-4-yl)imidazo[2,1-b][1,3,4]thiadiazole derivatives of the general formula (I) where: R5 is a hydrogen atom or a C1-3 alkyl, -NR7R8, or C1-3 alkyloxy group; R6 is an optionally substituted phenyl group; A is a C1-7-alklene group optionally substituted by one or two Ra groups; B is a C1-7-alkylene group optionally substituted by an Rb group; L is a nitrogen atom optionally substituted by an Rc or Rd group, or a carbon atom substituted by a Rei group and a Rd group or two Re2 groups; R7 and R8 are independently a hydrogen atom or a C1-3 alkyl group. The invention also relates to a method for preparing same and to the therapeutic use thereof.
US20130266508 Thermosensitive hydrogel for coating radioisotope and chemotherapeutic agent to treat cancer and method for preparing the same A thermosensitive hydrogel for coating radioisotopes and chemotherapeutic agents to treat cancer and a method for preparing the same are revealed. The anticancer drugs such as radiopharmaceuticals or chemotherapeutic agents are coated with the hydrogel formed by PCL-PEG-PCL. By the feature of the hydrogel body that changes from liquid phase at low storage temperature to gel form at body temperature, not only the anticancer drugs can be injected into the human body and reaching the treatment site smoothly but the treatment time of brachytherapy is also extended. Thus the side effects of cancer therapy are significantly reduced.
US7504098 Method for introducing a biological molecule using a viral envelope and heparin and system therefore The object of the present invention is to provide a method of efficient delivery into a brain and central nervous system, and to provide a method of efficient delivery with a viral envelope. The present invention provides a system for introducing a biomolecule into a cell comprising A) a biomolecule; B) a viral envelope; and C) glycosaminoglycan. Further, the present invention provides a method for delivering a biomolecule into a brain, comprising the steps of: A) transiently closing an artery of the head portion or cervical portion; and B) introducing a biomolecule into the brain during the closing of the artery of the head portion or the cervical portion.
CA2840875A1 Pharmaceutical composition for inflammatory diseases, allergic diseases and autoimmune diseases The present invention relates to a method and a pharmaceutical composition for suppressing immunity, in each of wherein a fatty acid derivative represented by general formula (I) is utilized. The present invention also relates to a method and a pharmaceutical composition for treating inflammatory diseases, allergic diseases and autoimmune diseases, in each of wherein the fatty acid derivative is utilized.
US8106035 For therapy and prophylaxis of cancer, dermatological disorders, bone disorders, thyroid disorders, wound healing and osteoporosis The present invention provides novel D-ring and side-chain analogs of 1α,25-dihydroxyvitamin D3, compositions comprising these compounds and methods of using these compounds as selective inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1α,25-dihydroxyvitamin D3, for example, cell-proliferative disorders.
CN101759598A Tetracycline compound with amino acid amidine The invention belongs to the technical field of medicines, and in particular relates to a tetracycline compound with amino acid amidine as shown in general formula (I), pharmaceutically acceptable salt or isomer thereof. In the general formula, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12 and n are as defined in the specification. The invention also relates to a preparation method of the compounds, a medicinal composition containing the compounds and an application of the compounds in the preparation of medicine for treating and/or preventing tetracycline-sensitive diseases, especially anti-infective medicine.
CN1919185A Compound ammonium glycyrrhizinato S dispersed tablet and its preparing process The invention discloses a compound ammonium glycyrrhizinate S dispersible tablet, wherein the dispersible tablet is prepared from the following raw materials (by weight portion): monoammonium glycyrrhizinate S (calculated by glycyrrhizinic acid) 5-30 parts, glycine 5-30 parts, DL-methionine 5-30 parts, bulking agent 55-220 parts, crumbling agent 32-160 parts, lubricating agent 0.2-5 parts. The dispersible tablet has the advantages of shorter disintegration time, better dispersion state, faster medicament dissolving, quicker absorption, and higher biological availability, thus is especially suitable for the elder people and patients suffering from swallowing difficulty.
US20110223246 Docosahexaenoic acid bound in phospholipids and method of recovering same from a natural source Medicaments and therapeutic compositions contain (1) phospholipids having 4,7,10,13,16,19-docosahexaenoic acid covalently bound thereto and (2) at least one omega-3 polyunsaturated fatty acid, or at least one pharmaceutically acceptable omega-3 polyunsaturated fatty acid derivative or mixtures thereof, wherein about 25% of the total 4,7,10,13,16,19-docosahexaenoic acid moieties in the composition are covalently bound to phospholipids, and wherein components (1) and (2) are present in amounts effective to support overall neurological health in a subject.
CN102030802A Adamantine amino tea sapogenol as well as preparation method and application thereof The invention discloses adamantine amino tea sapogenol as well as a preparation method and application thereof. The adamantine amino tea sapogenol has a structure shown as a formula I and can be prepared by the following steps of: reacting triphenyl chloromethane with tea saponin element and connecting triphenylmethyl to a primary hydroxyl of the tea saponin element C28; reacting acetic anhydridewith the tea saponin element and connecting acetyl to a secondary hydroxyl of the tea saponin element; adding a triphenylmethyl protective agent and reacting with the tea saponin element to remove the triphenylmethyl on the tea saponin element; reacting and connecting the tea saponin element with adamantine under the condition that a catalyst exists; and finally, adding an acetyl deprotection agent to remove the acetyl on the tea saponin element and obtaining the adamantine amino tea sapogenol shown as the formula I by crystallization. The invention has the advantages of simple preparation process, mild reaction conditions and high purity of products and can be used for industrial production; and the obtained adamantine amino tea sapogenol has a small structure and the protective activityof the adamantine amino tea sapogenol on nervous centralis is remarkably improved.
US20090075973 Benzo-fused heterocycles The present invention provides benzo-fused heterocyclic compounds having the structure of formula I, as well as prodrugs, stereoisomers, racemates, salts, hydrates, solvates, acid salt hydrates and isomorphic crystalline forms thereof. The compounds directly or indirectly modulate the activity of one or more cannabinoid receptors and can be incorporated into pharmaceutical preparations that are useful for the prevention and treatment of a variety of diseases and conditions, including pain, inflammation and pruritis.
EP1968978A2 Forms of dolasetron mesylate and processes for their preparation The present invention provides crystalline polymorphic forms of Dolasetron mesylate. Also provided are methods of preparing the crystalline polymorphic forms of Dolasetron mesylate. Further, the crystalline Dolasetron mesylate forms may be used in pharmaceutical compositions.
WO2009122180A1 Pyrimidine derivatives capable of inhibiting one or more kinases A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, formula (I): wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycIoalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, -NR4R5, -OR6, -NR7(CO)R6, -NR7(CO)NR4R5, -NR7SO2R6, -NR7COOR7, -CONR4R5, C3-6-heterocycloalkyl and formula (a, b, c): wherein R4-7 and A are as defined in the claims. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.
EP2473199A1 Isotopically labeled neurochemical agents and uses thereof for diagnosing conditions and disorders The invention relates to a neurochemical agent comprising at least one isotopically labeled carbon atom directly bonded to at least one deuterium atom, uses thereof for the manufacture of a composition for diagnosing and evaluating a condition or disease and kits comprising said agent. The invention further encompasses methods for diagnosing and evaluating a condition or disease in a subject utilizing a composition of the invention.
US20100313285 Altering High Density Lipoprotein Levels Through UDP-N-Acetyl-Alpha-D-Galactosamine: Polypeptide N-Acetlgalactosaminyltransferase (GALNT) Modulation Described herein are methods for detecting and treating coronary artery disease and atherosclerotic conditions based on modulating the levels of total plasma lipoprotein and HDL-C by inhibiting expression or activity of GALNT. Also described herein are methods for identifying an agent(s) useful in treating coronary artery disease or atherosclerotic conditions.
WO2012162468A1 Thiazol derivatives as pro -matrix metalloproteinase inhibitors This invention relates to methods for preventing, treating or ameliorating an MMP9 and/or MMP13 mediated syndrome, disorder or disease comprising administering to a subject in need thereof an effective amount of a thiazol derivative such as a compound listed in the examples section of this specification, or a form, composition or medicament thereof. Disorders treated and/or prevented include rheumatoid arthritis.
CN102579800A Phenformin hydrochloride and preparation process thereof The invention relates to a compound phenformin hydrochloride and a preparation process thereof. The compound phenformin hydrochloride is prepared from the following raw materials in parts by weight: 1 part of phenformin hydrochloride, 25 parts of membranous milkvetch root, 22 parts of Chinese yam, 20 parts of Chinese atractylodes, 15 parts of figwort, 10 parts of Chinese angelica and 7 parts of dwarf lilyturf turber. The compound phenformin hydrochloride can be produced into capsules, tablets, granules and other formulations by adding pharmaceutical excipients, such as starch and edible cellulose according to an ordinary pharmacy method. A compound phenformin hydrochloride pharmaceutical composition disclosed by the invention has the advantages of treating both manifestation and root cause of diabetes, being non-toxic and harmless to a human body, having no side effect, being low in price, being simple and convenient to manufacture and having broad application prospects.
US20120208855 Amino-benzoic acid derivatives for use in the treatment of dihydrogenase-related disorders Provided herein is method of modulating, and in particular decreasing dihydroorotate dehydrogenase (DHODH) activity, as well as a method of treating a DHODH related disease or disorder.
CN102858349A Pharmaceutical Composition For The Treatment Of Alzheimer's Disease, Method For Producing Same And Use Thereof The present invention relates to the use of microdoses of lithium compounds for the treatment of Alzheimer's disease. The results show that the administration of lithium microdoses provides an alternative proven to be not toxic for elderly people, for slowing down or stopping the progression of the disease and the progressive cognitive deterioration.
WO2010123527A3 Use of epidermal growth factor inhibitors in the treatment of viral infection The present invention provides methods of treating a viral infection in an individual. The methods generally involve administering to an individual an effective amount of an epidermal growth factor receptor (EGF-R) inhibitor.
US7605181 Method for the treatment of metabolic disorders Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. wherein n is 1 or 2; m is 0, 1, 2, 4, or 5; q is 0 or 1; t is 0 or 1; R2 is alkyl having from 1 to 3 carbon atoms; R3 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; and R1 is hydrogen or alkyl having 1 or 2 carbon atoms. Alternatively, when R1 is hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula I.
CN103432147A Oral medicinal preparation containing glycosyl modified polyphenolic substance and application of oral medicinal preparation The invention discloses an oral medicinal preparation containing a glycosyl modified polyphenolic substance. Each unit dosage of the oral medicinal preparation contains 1-200mg of glycosyl modified polyphenolic substance, wherein the unit dosage is the total amount of the medicinal preparation used each day. The glycosyl modified polyphenolic substance can be combined with other medicaments or used independently, can be added with a pharmaceutically acceptable medical carrier to enable the glycosyl modified polyphenolic substance to account for 0.5-60 percent of the total weight of the medicinal preparation, and tablets, pills, capsules, granules, suspension, aerosol, oral solutions and sustained-release preparations can be prepared. The invention also provides applications of the medicinal preparation in preparing weight-reducing medicines, weight-reducing health-care products, blood-fat reducing medicines and blood-fat reducing health-care products. The oral medicinal preparation containing the glycosyl modified polyphenolic substance is good in water solubility, can be used for treating obesity with a remarkable weight-reducing effect, in particular treating obesity caused by diet, heredity and reduction of metabolism, can be used for treating hyperlipidemia with a remarkable blood-fat reducing effect, and has a wide application prospect.
WO2013041472A1 Triazolopyridine compounds as pde10a inhibitors The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2 and R3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
CN102858743A Spiro-condensed cyclohexane derivatives as HSL inhibitors useful for the treatment of diabetes Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions as HSL inhibitors for the treatment of diabetes, wherein R1,R2, R3, Ca and Cb have the significance given in claim 1.
US20130023554 5-phenylpyrazolopyridine derivatives, preparation and therapeutic use thereof Compounds of formula (I): in which: R1 represents a phenyl group or naphthyl group, optionally substituted by one or more atoms or groups chosen, independently of one another, from: halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, (C1-C6)thioalkyl, —S(O)(C1-C6)alkyl, —S(O)2(C1-C6)alkyl, hydroxyl, hydroxy(C1-C6)alkylene, CHO, COOH, (C1-C6)alkoxy(C1-C6)alkyleneoxy, NRaRb, CONRaRb, SO2NRaRb, NRcCORd, OC(O)NRaRb, OCO(C1-C6)alkyl, NRcC(O)ORe or NRcSO2Re; X represents from 1 to 4 substituents which are identical to or different from one another and which are chosen from hydrogen, halogen, (C1-C6)alkyl or (C1-C6)alkoxy, it being possible for the (C1-C6)alkyl to be optionally substituted by one or more groups chosen from a halogen, (C1-C6)alkoxy or hydroxyl; R2 and R3 represent, independently of one another, a hydrogen atom, a (C1-C6)alkyl group optionally substituted by an Rf group, or a CHO or COOH group; X and R3 can together form, with the carbon atoms which carry them, a carbocycle of 5 to 7 carbon atoms; R4 represents a hydrogen atom or a (C1-C6)alkyl group; Ra and Rb represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl, aryl(C1-C6)alkylene or aryl group; or Ra and Rb together form, with the nitrogen atom which carries them, an azetidine, pyrrolidine, piperidine, azepine, morpholine, thiomorpholine, piperazine or homopiperazine group, this group being optionally substituted by a (C1-C6)alkyl, aryl or aryl(C1-C6)alkylene group; Rc and Rd represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl, aryl(C1-C6)alkylene or aryl group; or Rc and Rd together form a (C2-C5)alkylene group; Re represents a (C1-C6)alkyl, aryl(C1-C6)alkylene or aryl group; or Rc and Re together form a (C2-C5)alkylene group; Rf represents a hydroxyl, oxo, CHO or COOH group, in the form of the base or of an addition salt with an acid. Therapeutic use and synthetic process.
EP0946508B1 NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
WO2011092840A1 Method for manufacturing polymethoxyflavones that are highly stable over time and have reduced residual pesticide levels Provided is a method for manufacturing inexpensive, highly safe, highly stable, versatile polymethoxyflavones that can be used in food products and easily incorporated into a variety of pharmaceutical formulations. Said method can, in one pass, isolate a large quantity of polymethoxyflavones from other components in a citrus peel oil. Also provided is a method for using said polymethoxyflavones. The provided method for manufacturing polymethoxyflavones from a citrus peel oil is characterized by the inclusion of: a step in which volatile components in a citrus peel oil are removed by distillation, yielding a distillation residue; a step in which said residue is distilled in a thin-film vacuum distillation device, yielding a fraction; a step in which an extract is extracted from said fraction using an aqueous ethanol solution; and a step in which insoluble oils are removed from said extract and the extract is then brought into contact with activated carbon and refined. This method produces polymethoxyflavones that are highly stable over time and have reduced residual pesticide levels.
US8575145 Triazolopyridine compounds as PIM kinase inhibitors Compounds of Formula (I), in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.
US20100152280 Modulation of sid-1 expression Compounds, compositions and methods are provided for modulating the expression of SID-1. The compositions comprise oligonucleotides, targeted to nucleic acid encoding SID-1. Methods of using these compounds for modulation of SID-1 expression and for diagnosis and treatment of diseases and conditions associated with expression of SID-1 are provided.
CA2846416A1 Tripartite bioactive composition providing anti-oxidant and anti-inflammatory effects with immune system and stem cell production enhancement The inventive tripartite composition is a combination of fucoidan, trans-resveratrol, and bovine colostrum in effective quantities, in the range of from 1 : 1.5: 1.5 to 1 : 10: 10 in weight percent. This composition provides antioxidant protection of cells against free radicals, strengthens the immune system, and enhances cellular function and stem cell population, thereby providing renewal and repair throughout the body. The inventive composition can be administered by capsules, but is preferably applied in liquid form to the oral cavity, such as by sublingual dropper or by intraoral spray. This sublingual, intraoral application method of administration provides maximum absorption, thus minimizing cost, avoiding inactive ingredients that are present in tablets and capsules, increasing consumer convenience, and eliminating stomach irritation.
WO2010015800A1 Chewable formulation comprising alginate, bicarbonate and carbonate The present invention relates to a solid, ingestible composition comprising a) an alginate; b) a bicarbonate; and c) a carbonate wherein the composition is in the form of a chewable core, a process for preparing said composition, and its use in the treatment of reflux oesophagitis, gastritis, dyspepsia or peptic ulceration or for use as a sustained releasing or targeted delivery composition.
EP2654742A2 Methods of improving cognitive function A method of improving cognitive function or treating cognitive dysfunction is provided. The method is based on activating a kainate receptor or a glutamate GluR6 receptor by kainate or a glutamate GluR6 receptor activator such as an agonist. Additionally, a method of enhancing a learning ability by activating a kainate receptor such as the glutamate GluR6 receptor via kainate or a glutamate GluR6 receptor activator such as an agonist is provided.
US7094770 Treating hepatitus B, C and D; AIDS; antiproliferative agents The present invention relates to a composition for and a method of treating hepatitis B virus (HBV) infection, hepatitis C virus (HCV) infection, hepatitis D virus (HDV) infection or a proliferative disorder in a patient using an effective amount of a compound selected from the group consisting of formulas [I]–[IV] below and mixtures of two or more thereof: wherein the substituents are as defined herein. Pharmaceutical compositions comprising these compounds in combination with other HBV, HCV, or HDV agents is also disclosed.
CN102199152A Heterocycle imidazoles phosphatide kinases inhibitor The invention discloses a heterocycle imidazoles phosphatide kinases inhibitor. The heterocycle imidazoles compound has a structural formula shown as formula I. X, Y, Z, Q are selected from C or N; R1 is selected from pyridyl or halogen, nitrile group, C1-C4 alkyl, C1-C4 alkyloxy substituted pyridyl, pyrimidinyl or C1-C4 alkyloxy substituted pyrimidinyl, quinoxalinyl, quinolyl or halogenated quinolyl, phenyl or C1-C4 alkyloxy substituted phenyl; R2 is selected from aromatic heterocycle which comprises pyridyl, naphthyl, phenyl, and disubstituted or monosubstituted pyridyl and phenyl, wherein the substituent is selected from a group of halogen, C1-C4 alkyl, or halogen, nitrile, imidazolyl or triazolyl substituted C1-C4 alkyl, C3-C10 cyclic hydrocarbon group, C1-C4 alkyl, C1-C4 sulfonyl, C1-C4 alkoxy, C1-C4 alcoxyl alkyl monosubstituted or disubstituted amido, or C1-C4 alkyl, C1-C4 sulfonyl substituted or non- substituted piperidino, 2- pyrrolidone group, C1-C4 alkoxyalkyl, imidazolyl, pyridyl, triazolyl; R3 is selected from O or S; R4 is selected from H, C1-C4 alkyl or C1-C4 alkyloxy; and R5 is selected from H or C1-C4 alkyl.
WO2008120653A1 Indoledione derivative A compound represented by the general formula (I-a): (I-a) [wherein R1a and R2a each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R3a means hydrogen, lower cycloalkyl, lower alkyl, etc.; R4a and R5a each means lower alkyl, lower cycloalkyl, etc. or R4a and R5a are bonded to each other to form lower cycloalkylidene; and R6a means lower alkyl, lower haloalkyl, etc.]. This compound functions as an LCE inhibitor and is useful as a therapeutic agent for various circulatory diseases, nervous diseases, metabolic diseases, reproductive diseases, digestive tract diseases, neoplasm, infectious diseases, etc.
CN102992988A Substituted phloroglucinol derivatives and application thereof The invention discloses a series of substituted phloroglucinol derivatives with a structure shown as the general formula (I) in the specification, and a pharmaceutically acceptable salt thereof, wherein in the general formula (I), A is selected from H, methyl, ethyl or propyl; B1 is selected from H, allyl or natural glycosides disaccharides; B2 and B3 are respectively selected from H or allyl; and X-Y represents that two carbon atoms are connected by a single bond or a double bond. The invention further provides a preparation method of the compounds, and applications of the compounds to preparation of drugs for improving the function of respiratory systems, in particular cough-relieving drugs. Experiments prove that the derivatives, disclosed by the invention, have remarkable cough-relieving effect, no clinical addiction, stable physicochemical property and good prospect as clinical cough-relieving medicine, and are simple in synthetic process and suitable for large-scale production.
WO2012064557A2 Deodorizing compositions Compositions that inhibit the generation of malodor-causing bacteria present in perspiration are disclosed.
US7119090 Anticancer agents; antiinflammatory agents; autoimmune diseases; rheumatic diseases, enzyme inhibitors The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
CN101343247A Cyclohexenone extract of Antrodia camphorata The invention relates to a novel compound as well as purposes thereof, particularly relating to 4-oxhydryl-2, 3-dimethoxy-6-methyl-5(3, 7, 11-trimethyl-2, 6, 10-dodecatriene)-2-cyclohexenone (4-hydroxy-2, 3-dimethoxy-6-methy-5(3, 7, 11-trimethyl-dodeca-2, 6, 10-trienyl)-cyclohex-2-enone) separated from an Antrodia camphorata extract as well as the applications thereof in inhibiting the growth of tumor cells. The compound in the invention is firstly found in Antrodia camphorata, and can be applied to the inhibition of growth of tumor cells of breast cancers, liver cancers and prostate cancers, meanwhile serving as an ingredient of pharmaceutical compositions for restricting the growth of the tumor cells, or being applied to the prevention of cardiovascular diseases or added to healthy beverage and food by further leveraging the oxidation resistance activity thereof.
CA2212888C A method for the treatment of hyperproliferative epithelial skin diseases by topical application of hydroxylated aromatic protein cross-linking compounds The present invention relates to a method of treating hyperproliferative epithelial lesions by topical administration. The method prevents growth and actively cross-links these aberrant cells, thereby killing the cells. The present invention is useful in control and prevention of hyperproliferative epithelial disorders, such as HPV-infected cell lesions, actinic keratosis, melanomas, and malignant and pre-malignant carcinomas.
WO2014139326A1 Pyrazolo compounds and uses thereof Provided are compounds useful as inhibitors of one or more histone demethylses, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.
US20120108604 Processes for preparing amine salts of sildenafil-analogues and use thereof A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R1, Ra and RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function.
CN103169716A Compound medicinal composition for treating pain The invention relates to a compound medicinal composition for treating pain, and in particular relates to a medicament composition. The compound medicinal composition comprises helicid, a compound shown in a formula I and an optionally pharmaceutically acceptable carrier, wherein R1 and R2 are independently selected from hydrogen and C1-6 alkyl, or a C3-8 naphthenic group formed by R1 and R2 and carbon atoms connecting R1 and R2, respectively. The compound medicinal composition can be used for treating and/or preventing pain, such as treatment and/or prevention of chronic neuropathic pain.
US20120046312 3-substituted propanamine compounds Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.
CN1613862A Adriacin derivative with anti-cancer activity This invention relates to farmiblastina derivatives, shown as formula, wherein: R1=H or OH, R2 and R3= H or C1-4 hydrocarbon, R4=H, C1-40 saturated or unsaturated hydrocarbon or XR5, wherein X=NH or O, R5=C1-40 saturated or unsaturated hydrocarbon, W=O or NH, R6=H, OH, or O(C1-4 hydrocarbon), R7=H or OH. The invention relates to its preparation and use as medicinal active component thereof.
CN102106857B Compound ceftiofur sodium freeze-dried power injection used for injection The invention is a compound ceftiofur sodium freeze-dried power injection used for injection, and the compound ceftiofur sodium freeze-dried power injection provided by the invention is mainly composed of the following effective components in parts by weight: 2-4 parts of ceftiofur sodium, 1 parts of sulbactam sodium and 1 parts of flunixin meglumine; a vacuum freeze drying method is adopted to prepare the effective components into the compound ceftiofur sodium freeze-dried power injection used for injection. The compound ceftiofur sodium freeze-dried power injection has the advantages that the preparation cost can be lowered, and the drug resistance of bacteria on the ceftiofur sodium is relieved; and the broad antimicrobial spectrum is wide, the activity is strong, the drug administration times is less, and low stress and slight side effect are endured; and the negative effect of endotoxin can be effectively blocked.
EP1746998A1 Combination therapy for lower urinary tract symptoms This invention relates to combination therapy for the treatment of benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) associated with or without BPH. The combination therapy comprises of 1a adrenergic receptor (AR) subtype selective antagonist in combination with muscarinic receptor antagonist and optionally included 5 -reductase inhibitor for relief of LUTS in a subject with or without BPH.
CN1739685A Compound isatis leaf-vitamin C prepn The compound isatis leaf-vitamin C preparation contains both isatis leaf extract and vitamin C, and may be in different forms, including capsule, chewing tablet, effervescent tablet, tablet and injection. The present invention facilitates the simultaneous taking of isatis leaf extract and vitamin C.
US8252322 Delivery system with increased bioavailability The present invention is directed to a dry composition which allows delivery of active agents with good bioavailability. These compositions are prepared by emulsifying the active agent using liposome technology known in the art and then encapsulating with a modified starch. The modified starch is prepared by enzymatic hydrolysis of starch after the preparation of a starch derivative containing a hydrophobic group or both a hydrophobic and a hydrophilic group. The resultant composition is a dry powder with excellent bioavailability. Further, the composition has good load levels and stability.
US8093256 Use of 8-substituted-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives The invention relates to use of substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. More specifically, the invention relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of GSK3β, such as Pick's disease among various other diseases as claimed herein.
EP1100454B1 Pharmaceutical compositions for managing skin conditions This application relates to a stable pharmaceutical composition and methods for the cleansing of skin to facilitate the prevention, treatment, and management of skin conditions, such as seborrheic dermatitis, psoriasis, folliculitis, rosacea, perioral dermatitis, acne, impetigo and other inflammatory skin conditions, and the like, including a sufficient amount of an acidic component of a hydroxyacid or tannic acid, or a pharmaceutically acceptable salt thereof, to exfoliate a portion of the skin, a sufficient amount of stabilized hydrogen peroxide to facilitate cleansing of the skin without substantial irritation thereof, and an antimicrobial agent in an amount sufficient to inhibit or reduce microorganisms on the skin.
CN1973840A Long acting slow releasing drug addiction eliminating prepn and its prepn process and use The present invention provides the preparation process and usage of slow released naltrexone (NTX) preparation, which is used in the rehabilitation after eliminating opium addiction. The NTX preparation includes NTX as the opium receptor antagonist and matrix of biodegradable polymer material polylactic acid. The preparation process includes emulsification and solvent volatilization to prepare microsphere, pressing into tablet, coating with polylactic acid and other steps. The NTX preparation has great medicine carrying amount and high encapsulating rate, and may reach blood medicine concentration for over 360 days. When it is used, the NTX preparation is injected with special injector into subcutaneous fat for NTX to release slowly and persistently to maintain the effective blood medicine concentration.
CN103610657A Acotiamide sustained-release preparation The invention provides an acotiamide sustained-release preparation. An acotiamide sustained-release part contains at least one high molecular polymer which is a sustained-release framework material, preferably hydroxypropyl methyl cellulose, methyl cellulose, hydroxypropyl cellulose, polyethylene oxide, hydroxyethyl cellulose, polyvinyl alcohol, polyvinyl pyrrolidone, acrylic acid copolymer and the like.
US20060188437 Isolation of a cell-specific internalizing peptide that infiltrates tumor tissue for targeted drug delivery The present invention provides a tumor-homing peptide that can target cancer and or tumor tissues. The peptide is uptaken by certain specific cancer cell types. The invention describes methods to achieve targeted delivery of anticancer drugs conjugated to this peptide for anticancer therapy. The invention also describes methods for using the peptide for the diagnosis and imaging of cancer and tumor tissues.
CN103239458A Application of 3, 20-dioxodinor friedelane in preparation of medicines for treating cancer The invention relates to an application of 3, 20-dioxodinor friedelane in preparation of medicines for treating cancer. The 3, 20-dioxodinor friedelane obtained by the invention has cytotoxic activity to cancer cell lines cultured in vitro, and is an effective anti-tumor medicine.
US20110166216 Compositions and Methods for Inhibiting Growth and Metastasis of Melanoma There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
CN103690507A Pulse sustained-release oral preparation and preparation method thereof The invention discloses a pulse sustained-release oral preparation and a preparation method thereof. The pulse sustained-release oral preparation includes a sustained-release tablet core and a time-lag coating layer. The sustained-release tablet core comprises a sustained-release drug pellet and tablet core auxiliary materials. The sustained-release drug pellet includes: 50-80% of a blank pill core; 2-10% of an expansion layer; 3-20% of a main drug layer; and 10-30% of a sustained-release coating layer. The preparation method comprises the steps of: (1) under stirring, adding the expansion layer, the main drug layer and the sustained-release coating layer into a benign solvent including water and/or alcohol of C1-C4 respectively, then wrapping the blank pill core with the layers, and collecting the formed sustained-release drug pellet; (2) mixing the sustained-release drug pellet with the tablet core auxiliary materials, and conducting direct compression to obtain the sustained-release tablet core; and (3) wrapping the sustained-release tablet core with the time-lag coating layer, thus obtaining the pulse sustained-release oral preparation. The pulse sustained-release oral preparation provided by the invention can realize rapid release and slow release of drugs by the same pellet, and has the advantages of stable absorption, high security, small individual difference, and small toxic and side effect.
EP1711473A1 Substituted n-cyclohexylimidazolinones having an mch-modulatory effect The invention relates to substituted N-cyclohexyl heterocycles as well as the physiologically acceptable salts and physiologically functional derivatives thereof, methods for the production thereof, and the use thereof as medicaments. Disclosed are compounds of formula (I), wherein the radicals have the indicated meanings, the physiologically acceptable salts thereof, and methods for the production thereof. Said compounds cause weight loss in mammals, for example, and are suitable for the prevention and treatment of obesity and diabetes, for instance.
WO2007089906A3 Cationic steroid antimicrobial compositions for treating or preventing herpes infections The invention provides methods for decreasing or inhibiting herpesviridae (HV) infection or pathogenesis of a cell in vitro, ex vivo or in vivo, a symptom or pathology associated with a herpesviridae (HV) infection or pathogenesis in vitro, ex vivo or in vivo, or an adverse side effect of herpesviridae (HV) infection or pathogenesis in vitro, ex vivo or in vivo. In one embodiment, a method of the invention includes treating a subject with an invention compound (e.g., cationic steroid antimicrobial or CSA).
CN103083312A Applications of Chinese starjasmine stem aglycon, burdock aglycon and Chinese starjasmine stem glucoside as dibenzyl butyrolactone compounds to preparation of medicaments for treating hepatitis viruses This invention relates to applications of Chinese starjasmine stem aglycon, burdock aglycon and Chinese starjasmine stem glucoside as dibenzyl butyrolactone compounds to the preparation of medicaments for treating hepatitis viruses and particularly hepatitis C viruses. The three compounds can be also used for preparing liver protection food or healthcare product. The invention provides the new applications of the Chinese starjasmine stem aglycon, the burdock aglycon and the Chinese starjasmine stem glucoside. The study on tests on resisting hepatitis C viruses shows that the three compounds have very significant hepatitis C virus resisting activity and can serve as the sources of novel active components for developing the medicaments for resisting hepatitis viruses, the liver protection food and the healthcare product.
US20100311695 Hydroxy-bisphosphonic acid derivatives as vector targeting bone tissue The present invention relates to hydroxy-bisphosphonic acid derivatives corresponding to general formula (I): in which: -n and m denote, independently of one another, an integer ranging from 1 to 4, —X denotes an oxygen atom or an N—R3 group, —R1 and R3 denote, independently of one another, a linear or branched C1 to C6 alkyl group, and —R2 denotes a residue of a molecule of therapeutic or diagnostic interest, or pharmaceutically acceptable salts of said derivatives, and also the method for the preparation thereof and the therapeutic or diagnostic use thereof.
CN102757510A Low-molecular weight schisandra chinensis polysaccharides and preparation method and application thereof The invention discloses low-molecular weight schisandra chinensis polysaccharides and a preparation method and an application thereof, and belongs to the technical field of medicine. The molecular weight of the polysaccharide component is 3.4*10<3> Da, and the monosaccharide composition is as follows: mannose:glucose:galactose=1:11.38:3.55; and the polysaccharide component contains (1-3)-alpha-glucan and has a tri-helix structure. The study of in vivo activity against liver cancer of SCPP11 polysaccharide component shows that the polysaccharide component is significantly active against liver cancer (HepG-2), can significantly inhibit growth of liver cancer, and can significantly enhance the autoimmunity and in vivo antioxidant activity of mice as compared with the 5-Fu. The water-soluble low-molecular weight schisandra chinensis polysaccharides have the advantages of definite active components and controllable quality, and can be used as a drug against liver cancer or a health-care product for improving immunity.
US20090196834 Tobacco alkaloid releasing chewing gum The invention relates to a tobacco alkaloid releasing chewing gum comprising tobacco alkaloid, gum base, and chewing gum ingredients, said gum base comprising elastomer and resin-compounds constituting an amount in the range of about 2 to 20% by weight of said chewing gum.
WO2014055055A1 Pharmaceutical composition of 1-adamantylethyloxy-3-morpholino-2-propanol or pharmaceutically acceptable salts thereof for the treatment of cerebrovascular disease and neurodegenerative diseases of the central nervous system A pharmaceutical composition for parenteral administration containing the active ingredient 1-adamantylethyloxy-3-morpholino-2-propanol, or pharmaceutically acceptable salts thereof, in a concentration range of from 3 to 100 mg/ml for the treatment of cerebrovascular disease.
CN101711857A Film coating agent for treating whitevein and preparation method thereof The invention discloses a medicine composition of a film coating agent for treating whitevein and a preparation method thereof. In the invention, the film coating agent is prepared and obtained by taking a recipe of the traditional Tibet medicine of a white vein ointment as a basic recipe through changing a medicament form. The invention adopts an ultramicro preparation method which extracts parts of medicinal materials by parts of medicinal materials, so that the effective components in the medicinal materials are effectively retained, the content of the components of crude medicines is greatly enhanced, the bioavailability is enhanced, and the curative effect is better. The film coating agent is smeared at an affected part, a layer of yellow brown film which is precisely attached to the affected part is formed after a solvent volatilizes, can be attached to the affected part for a long time and becomes a medicine carrier, the aim of slow release of the medicines is achieved, and the acting time of the effect of the medicines is long and lasting. Because the film formed at the affected part by the film coating agent is insoluble in water, the film can not be washed by the water; in addition, because the film has large plasticity, can not crack and can be conveniently torn off when being not needed, the film does not influence the normal life of a patient.
CN101283989A Metronidazole vaginal tablet process and quality control method The invention relates to a preparation method and a quality control method of a new gynecologic drug, Metronidazole, Clotrimazole and Chlorhexidine Acetate Vaginal Tablets, with antibacterial and anti-inflammatory effects. The added lactic acid-calcium lactate buffer system results in a drug with pH of 3.5-4.0 t that is similar to the physiological pH in vagina, so as to effectively retain physiological environment in vagina, provide existing conditions suitable for vaginal beneficial bacteria, and promote rehabilitation. The main preparation method comprises the steps of compounding, granulating, grading, mixing, and tabletting. The quality control method comprises the steps of collecting one dosage unit of the product, grinding, adding 100mL water, shaking for 10min, and testing pH (should be 3.5-4.0); testing melting time limit (should be 30min); and measuring the nominal content of the three components by high performance liquid chromatography (should be both in the range of 90.0-110.0%).
US20080194476 Medicament Comprising A Peptide Extract Of Avocado, Which Is Intended For The Treatment And Prevention Of Illnesses That Are Linked To An Immune System Deficiency The invention relates to a medicament which comprises a peptide extract of avocado and which can also comprise a composition containing D-mannoheptulose and/or perseitol, such as a water-soluble extract of avocado sugars, and/or a peptide extract of lupine. The inventive medicament is intended for the treatment and/or prevention of illnesses that are linked to an alteration in innate and/or acquired immunity, through an increase in the production of anti-microbial peptides, preferably hBD-2, without inducing inflammatory reactions, irritations or intolerances.
WO2014016361A1 Multimeric mannosides, a process for preparing the same and their uses as a drug The present invention relates to multimeric mannosides, a process for preparing the same and their uses in medicine for treating Escherichia Coli infections. Exemplary compounds are:
WO2013117749A1 Pyrrolic derivatives, processes for preparing the same and their uses as a drug The present invention relates to pyrrolic derivatives I, processes for their preparation, and their use as new antibacterial drugs.
CN103721106A Method for preparing washing paste for treating acnes The invention discloses a method for preparing washing paste for treating acnes and aims to provide washing paste for treating acnes. According to the adopted technical scheme, the acne washing paste is prepared from orris root, glutinous rice flour and alums. The technical scheme adopted in the invention is easy and convenient to operate, the washing paste for treating acnes is capable of quickly cleaning off acne dirt, and cell regeneration of affected parts is promoted.
EP2726470A1 1, 2, 4 -thiadiazol- 5 -ylpiperazine derivatives useful in the treatment neurodegenerative diseases The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
WO2013126776A1 Nanostructures for treating cancers and other conditions Nanostructures, compositions and methods for treating cancers and other conditions are provided. In some cases, the nanostructures and/or compositions may be used to treat cancers or other diseases or conditions at least in part by controlling cholesterol metabolism in cells. The nanostructures and compositions may be used, for example, to control cholesterol influx and/or efflux in cells. In some cases, the nanostructures or compositions may be used to kill the cells. Examples of cancer cells that may be affected by the nanostructures and compositions described herein include those having scavenger receptor type B-I (SR-B1), B-cell lymphoma cells, non-Hodgkin's lymphoma cells, melanoma cells and/or others. In some embodiments, the nanostructures may be mimics of natural high-density lipoprotein (HDL).
US6929012 Process for the isolation of a major harmful oxidant from cigarette smoke The components of cigarette smoke, known until now, do not explain the overwhelming hazardous effects of smoking; this invention describes the isolation, identification and procedures for determination of the structure, properties and assay of a relatively stable major harmful oxidant (cs-oxidant) present in the cigarette smoke, the content of which is about 190±10 μg per cigarette; the cs-oxidant alone almost quantitatively accounts for the oxidative damage of proteins produced by the aqueous extract of whole cigarette smoke, it is also responsible for the oxidative damage of DNA; since the cs-oxidant is relatively stable, it further explains the deleterious effects of the side stream smoke and passive smoking; a number of chemical compounds/agents including vitamin C have been found to prevent the cs-oxidant induced protein oxidation in vitro.
CN1759832A Carbazochrome sodium sulfonate for injection, and preparation method An injection of carbazochrome sodium sulfonate is prepared from carbazochrome sodium sulfonate (0.9-1.1 Wt%), antioxidizing agent (0.01-0.5), pH regulator (0.01-0.5) and the water for injection (98.2-99).
EP1478364B1 Selective antibacterial agents The present invention relates to the use of compounds of the general Formula (I), for the regulation of the quorum sensing system of microorganisms wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A?1 and A2¿ each independently represent an optionally substituted C¿1?-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR?4¿, CO, CO¿2?, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR?4¿, SO or SO¿2?; said substituted ring system carries a substituent R?3¿ on one or more of the carbon atoms of said ring system;said substituted C¿1?-C20-alkyl group carries a substituent R?3¿ on one or more of the carbon atoms of said alkyl group; R3 is independently H, OR4, SR4, hydroxyalkyl, hydroxyalkylamino, cycloalkyl, halogen, haloalkyl, haloalkyloxy, NO¿2?, CN, SO2NR?4R5, CO¿2NR?4R5, COR4, CO¿2R4, SO2R4, SO3R?4, NR4R5¿, alkyl, aryl or heteroaryl; R4 is H, alkyl, cycloalkyl, aryl or heteroaryl; R5 is H, O-alkyl, O-aryl, alkyl, heteroaryl or aryl; Y?1 and Y2¿ are independent from each other C=O, C=S, SO2 or C=NR5; p is 0, m is 0, n is 0; or p is 0, m is 0, n is 1;or p is 0, m is 1, n is 1; or p is 1, m is 0, n is 0; or p is 1, m is 0, n is 1; or p is 1, m is 1, n is 1.
WO2009007814A1 Inhibitors of carbonic anhydrase The invention relates to a compound of formula (I) and to pharmaceutically acceptable salts and solvates thereof. The invention also relates to methods of treating glaucoma, ocular hypertension, age-related macular degeneration, diabetic macular edema, diabetic retinopathy, hypertensive retinopathy, retinal vasculopathies and intraocular pressure in mammals by administering the compound, and to pharmaceutical compositions which contain the compound for such treatments. The invention also relates to methods of preparing the compound.
WO2010019435A3 Solid states of atorvastatin potassium Atorvastatin potassium crystalline Forms A, B, E, F, and G are provided. Also provided are methods of preparing atorvastatin potassium crystalline Forms A, B, E, F, and G. Atorvastatin potassium crystalline Forms A, B, E, F, and G may be used to prepare pharmaceutical compositions useful for the treatment of hypercholesterolemia or hyperlipidemia.
US20100297235 Vascular puncture closure systems, devices, and methods using biocompatible synthetic hydrogel compositions A hydrogel composition for application to vascular puncture site of an animal to arrest bleeding and promote hemostasis mixes a biocompatible, synthetic, electrophilic polymer component comprising a poly(ethylene glycol) (PEG) Succinimidyl Glutarate having a functionality of four and a molecular weight of about 10,000 g/mole, with a biocompatible, synthetic, nucleophilic polymer component comprising a blend of a poly(ethylene glycol) (PEG) Amine having a functionality of four and a molecular weight of about 10,000 g/mole, and a Poly-L-Lysine hydrobromide having a molecular weight of greater than about 8000 g/mole.
US20100280053 CyclopropylmethYl-[7-(5,7-dimethyl-benzo[1,2,5]thiodiazol-4-yl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-4-propyl-amine as a CRF Antagonist The present invention relates to a novel benzothiadiazole of formula (A) in free base or acid addition salt form, its preparation, its use as pharmaceutical and pharmaceutical compositions containing the compound.
US20110178131 Compounds Which Have Activity At M1 Receptor And Their Uses In Medicine Compounds of formula (I) or a salt thereof are provided: wherein R4, R6, R7, R8, Q, A, Y, n and R are as defined in the description. Use of the compounds for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
WO2013174997A1 Methods and pharmaceutical compositions for the treatment of refractory haematological malignancies The present invention relates to methods and pharmaceutical compositions for the treatment of refractory haematological malignancies. More particularly, the present invention relates to an inhibitor of pyruvate dehydrogenase kinase 1 (PDK1) activity or expression for the treatment of refractory haematological malignancy in a subject in need thereof. PDK1 inhibition by DCA induces p53 expression. In wt p53 leukemias, DCA treatment sensitizes the tumor cells to conventional chemotherapy. In mutant p53 leukemias, DCA sensitizes tumor cells against HSP90 inhibitors.
EP2627635A1 Salts of arylsulfonamide ccr3 antagonists Provided herein are arylsulfonamide salts, e.g., a salt of a compound of Formula I, which are useful for modulating CCR3 activity, and their pharmaceutical compositions. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
US6919208 Methods and compositions for enhancing the delivery of a nucleic acid to a cell The present invention relates to methods and compositions useful for enhancing the efficiency of delivery of a nucleic acid to a cell. Preferably the cell is a mammalian cell. The method comprises providing to a cell an agent capable of enhancing the cytoskeletal permissiveness of the cell for transfection. The method also comprises providing to the cell a nucleic acid delivery system for the transfection of the cell, whereby the efficiency of delivery of a nucleic acid to the cell is enhanced. Compositions and kits for enhancing the efficiency of delivery of a nucleic acid to a cell are also included
WO2013139882A1 Pyrazolopyridines for treatment of parkinsons disease The invention relates to a compound of formula (1A) or (1B), or a pharmaceutically acceptable salt thereof, Wherein R1 is a group selected from alkyl, monocyclic heterocycloalkyl, bicyclic heterocycloalkyl and cycloalkyl, each of which is optionally substituted by one or more groups selected from alkyl, halo and cycloalkyl; for formula (1A): one, two or three of X1, X2, X3 and X4 are N, and the remainder are each independently CR2; or for formula (1B): X4 is C or N; and one or two of X1, X2and X3 are independently selected from N and NR8, and the remainder are each independently CR2; such that X1, X2,X3,X4and N form a heteroaryl group; each R2 is independently selected from H, alkyl, CN, halo, heteroaryl, heterocycloalkyl, cycloalkyl, OR4, CONR5R6 and SO2R7, wherein said alkyl, heteroaryl, heterocycloalkyl and cycloalkyl groups are each optionally further substituted by one or more groups selected from alkyl, halo and OR9; each R8 is independently selected from H and alkyl, wherein said alkyl group is optionally further substituted by one or more groups selected from CN, halo, heteroaryl, heterocycloalkyl, cycloalkyl, OR4, CONR5R6 and SO2R7; R4, R5, R6, R7and R9 are each independently selected from H and alkyl; or R5 and R6 together with the nitrogen to which they are attached are linked to form a cyclic group which optionally further comprises one or more heteroatoms selected from O, N and S; with the proviso that when the compound is of formula (IB), the compound is other than 3-(5-isopropyl-4H-1,2,4-triazol-3-yl)-N- (tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[4,3-c]pyridin-4-amine or 3-(5-cyclopropyl-4H-,2,4-triazol-3-yl)-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[4,3-c]pyridin-4-amine. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (1A) and (1B).
EP2058332A1 Use of CD25 binding molecules in steroid-resistant patients A method for the treatment of a disease selected from the group consisting of autoimmune hepatitis, eczema, vasculitis, temporal arteritis, sarcoid and Crohn's disease, in a steroid-resistant or steroid-sensitive patient, comprising administering to the patient in an effective amount of a CD25 binding molecule.
CN101926999B Hemostatic disinfectant and preparation method thereof The invention provides a hemostatic disinfectant. The solution of the hemostatic disinfectant comprises 0.1 to 50 mu m/ml hemostatic biological enzyme, a disinfectant of which the concentration can achieve sterilization and disinfection effects and 1 to 100 mg/ml protein protective agent. The hemostatic disinfectant is more suitable for cleaning and disinfecting the wound surface of skin, a mucous membrane or a tissue in surgical operation, stopping bleeding for a traumatic wound and disinfecting the traumatic wound. The invention also provides a method for preparing the hemostatic disinfectant. The preparation method comprises the following step of: preparing the solution of the hemostatic disinfectant which comprises 0.1 to 50 mu m/ml hemostatic biological enzyme, the disinfectant of which the concentration can achieve the sterilization and disinfection effects and 1 to 100 mg/ml protein protective agent.
WO2014068553A1 Aptamers, multimeric aptamers and uses thereof Monomeric and multimeric aptamers are provided. Also provided are pharmaceutical compositions which comprise same and methods of using same.
WO2006046915A1 Use of unsaturated quionoline or naphtalene derivatives as medicaments A compound of formula (I): (I), or a pharmaceutically acceptable salt thereof; for use as a medicament (for example modulating the glucocorticoid receptor in a warm blooded animal), and pharmaceutical compositions comprising such compounds.
US6949542 Dihydro-benzo[b][1,4]diazepin-2-one derivatives This invention relates to dihydro-benzo[b][1,4]diazepin-2-one derivatives of the formula wherein R1, R2, X and Y are as defined in the specification and R3 is a six-membered aromatic heterocycle containing 1 to 3 nitrogen atoms or a pyridine-N-oxide as further defined in the specification. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders.
CA2206748C Salts of ethyl 3-(2-(4-(4-(amino-imino-methyl)phenyl)-4-methyl-2,5-dioxoimidazolidin-1-yl)acetylamino)-3-phenylpropionate The present invention relates to ethyl 3-(2-(4-(4-(amino-imino-methyl)--phenyl)-4-methyl-2,5-dioxoimidazolidin-1-yl)acetylamino)-3-phenyl--propionate salts of the formula I, (see formula I) in which HB is maleic acid, and the physiologically tolerated salts thereof, to processes for their preparation and to their use in pharmaceuticals.
US7169559 Using low density lipoprotein related proteins (LRP) to diagnose, treat and prevent paget's, osteoporosis, cirrhosis and rickets LDL receptor-related proteins 1 and 2 (LRP-1 and LRP-2) and interaction between lactoferrin and LRP-1, LRP-2, or p42/44 MAP kinase in diagnosis and treatment of disorders such as bone or cartilage disorders. Also disclosed are methods of screening for related therapeutic compounds.
CN103145598A Oxaceprol crystal and composition comprising same The invention relates to an oxaceprol crystal and composition comprising the same. The characteristic peaks in an X-ray powder diffraction pattern of the oxaceprol crystal measured by Cu-K[alpha] rays are shown at 2[theta] of 4.8 degrees, 6.6 degrees, 11.2 degrees, 12.6 degrees, 14. 6 degrees, 15.5 degrees, 17.8 degrees, 19.1 degrees, 20.1 degrees, 21.5 degrees, 23.9 degrees, 27.2 degrees, 30.5 degrees and 33.2 degrees. Dissolvability tests show that the crystal reduces solubility in water at a certain degree. The crystal can be further used for preparing pharmaceutically acceptable tablets such as sustained release tablets. Since the solubility in water of the crystal is reduced, drug release behavior of the sustained release tablets prepared by the crystal is improved significantly, and stability of the sustained release tablets prepared by the crystal is more excellent.
EP2373315A2 Methods and compositions related to targeting monoacylglycerol lipase This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.
CN1634097A Application of C21 steroid glycoside in pharmacy The invention discloses the use of C21 steroid glycoside in pharmacy, wherein the systematic test shows that C21 steroid glycocide has low toxic and side effect, but has unique effect for treating psychogenia diseases with depression state, in particular for depression.
EP2763662A1 Pharmaceutical compositions of antihypertensives The present invention describes antihypertensive pharmaceutical formulations particularly formulations of losartan and indapamide.
CN102210650A Prednicarbate emulsifiable paste and preparation method thereof The invention discloses Prednicarbate emulsifiable paste, which is prepared from the following raw materials and auxiliary materials: 0.05 to 0.15 percent of Prednicarbate and 10 to 30 percent of pegoxol-7-stearate. In the invention, the pegoxol-7-stearate is used for preparing the Prednicarbate emulsifiable paste, low-speed stirring is used in a preparation process, and thus, the Prednicarbate emulsifiable paste which meets quality requirements of Chinese pharmacopoeia on emulsified paste in terms of fineness and particle size and has high coating performance is prepared; and the control in a production process is easy, so the Prednicarbate emulsifiable paste is more suitable for industrial production. The Prednicarbate emulsifiable paste disclosed by the invention can resist high temperature and is insusceptible to oil and water separation; the prepared emulsifiable paste has high stability at a temperature as high as above 40 DEG C, and is insusceptible to oil and water separation even at a temperature as high as above 60 DEG C; therefore, the emulsifiable paste is more stable than Prednicarbate emulsifiable paste prepared by the conventional process.
CN102225940A Isosorbide benzoate compound as well as preparation method and medicinal use thereof The invention relates to the fields of pharmaceutical chemistry and pharmacotherapeutics, and in particular relates to an isosorbide benzoate compound (I). The compound can be used for preparation of medicaments for preventing and treating ischemic cardiovascular and cerebral vascular ischemic diseases, medicaments for improving cardiovascular and cerebral circulatory disorder diseases and medicaments for resisting platelet aggregation, thrombo, dementia, diabete and complications thereof. The invention also relates to a preparation method of the compounds and a pharmaceutical composition containing the compounds.
CN101390824A Medical composition containing meptazinol hydrochloride The invention discloses a stable oral-taking solid medicine combination which contains meptazinol with effective treatment dosage, salt, organic acid and medicinal auxiliary material. The stable oral-taking solid medicine combination is used for the clinical treatments of intermediate pain, trauma, postoperative pain, obstetrical pain and renal colic.
WO2010036629A2 Fused multicyclic compounds as protein kinase inhibitors Fused multicyclic compounds of formula (I) defined herein are disclosed. Also disclosed are a method for inhibiting protein kinase (e.g., Aurora kinase) activity and a method for treating a protein kinase mediated disorder (e.g., cancer) with these compounds.
US20050267152 Gly1 transporter inhibitors and uses thereof in treatment of neurological and neuropsychiatric disorders The present invention relates to glycine transporter inhibiting compounds of formula (I): for treating disorders mediated by GlyT1, wherein R1—R9 are as in the description.
CN101829233A Smoking stopping agent composition and preparation method thereof The invention relates to a smoking stopping agent composition and a preparation method thereof. The smoking quitting agent composition is prepared by using the following raw materials by mass: 1 to 3 g of dry tobacco tar, 8 to 12 g of cordate houttuynia, 3 to 5 g of liquorice, 8 to 12 g of earthworm, 10 to 20 g of polygala and 0.2 to 0.6 g of butylparaben. The smoking stopping agent has the characteristics of rapid smoking cessation, little side effect, high effective rate, low cost, low relapse rate and good curative effect on patients with different smoking years.
US20120263675 Bivalent diazo bicyclic smac The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.
US20120264823 Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use The invention relates to compounds of Formula (I): (A′)x-(A)-(B)—(Z)-(L)-C(═O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A′), if present, is indepedently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2 or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.
CN1778824A Multiple homogeneous tremella polysaccharide, its extraction and medicinal composition with this compound as active components Several homogeneous tremella polysaccharides, its extraction and medicinal composition as the compound as active ingredient are disclosed. The process is carried out by boiling tremella spore fermentative, depositing by alcohol, gradient extracting by different concentration NaOH solution, column chromatography separating, purifying to obtain base-extracted tremella polysaccharide ATF-A, ATF-B, ATF-C and water-extracted tremella polysaccharide WTF-A and WTF-B, and mixing homogeneous tremella polysaccharide with medicinal accessory material to obtain various preparations. It can decrease immunity, delay senility and have antineoplastic and radiation-resistant functions.
US20090247508 Benzoimidazole Compounds Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
EP1381431B1 Aromatase inhibition to enhance implantation rate The use of at least one aromatase inhibitor in the production of a medicament for improving the implantation and pregnancy rates for a female undergoing assisted reproduction treatment, which comprises one or more daily doses of an aromatase inhibitor (AI) for administration during assisted reproduction cycles or ovarian stimulation cycles, wherein the doses of AI are selected from amounts effective to reduce serum estradiol levels. Also disclosed are related pharmaceutical preparations and packages.
CN102485232A Medicinal composition containing decitabine The invention discloses a medicinal composition containing decitabine. The composition comprises decitabine, a stabilizing agent and an excipient according to a weight ratio of 1:1-3:1-9. The medicinal composition which overcomes disadvantages of instability and easy degradation of decitabine has the characteristics of containment of decitabine, stability, and common and easily available auxiliary material. The medicinal composition can be used to treat the myelodysplastic syndrome (MDS).
CN103073608A Androstane-4, 6, 8 (9), 13 (14)-tetraene-3, 11, 16-triketone and application thereof The invention discloses a polyene high-oxidation androstane compound, i.e., androstane-4, 6, 8 (9), 13 (14)-tetraene-3, 11, 16-triketone. The compound is extracted from epigynum auritum plant. Experiments prove that the compound has an obvious suppression effect on Balb/c mouse spleen lymphopoiesis stimulated by ConA (concanavalin) and has activity equivalent to that of the conventional immunosuppression active substances, i.e., triptolide and dexamethasone.
US20130005804 Novel Uses of Neuraminidase Inhibitors in Infectious Diseases The present invention relates to methods of decreasing the infectivity, morbidity and rate of mortality, in treating diseases associated with a variety of pathogenic organisms, specifically diseases involving one or more pathogens that require neuraminidase as a virulence factor. In addition, the present invention uses biology based therapy to treat neuraminidase dependent infections or diseases dependent on sialic acid metabolism.
US8198292 Vinpocetine and eburnamonine derivatives for promoting bone growth, treating renal damage and cancer, and devices thereof The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The compounds include the salts, hydrates and isomers thereof. The present invention also provides methods for the treatment of renal disease and cancer.
EP1611104B1 Tetrahydroisoquinolyl acetamide derivatives for use as orexin receptor antagonists The invention relates to novel acetamide derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
CN201581012U Acid electrolyzed water disinfectant sterilizer The utility model discloses an acid electrolyzed water disinfectant sterilizer and relates to an acid oxidizing water generator which consists of a shell (1) and an internal device (2); the internal device (2) is arranged inside the shell (1); and an electrolytic bath provided with an aseptate platinum-titanium alloy electrode is adopted to electrolyze tap water comprising electrolyte and generate disinfectant with an oxidation-reduction potential of 1,150 plus or minus 50mv, a pH of 2.2 plus or minus 0.2 and effective chlorine content of 60 plus or minus 10mg/L, which can kill enteropathogenic bacteria, pyogenic coccus, pathogenic yeast and spores of bacteria, can sterilize live hepatitis B virus, has no poison and thrill to human bodies, has no pollution to skin mucous membrane, and has no pollution to the environment; moreover, sterilized raffinate can be automatically reduced to fresh water automatically after being discharged.
US20100183748 Methods for Treating or Preventing Radiocontrast Agent Induced Kidney Injury Methods for treating or preventing radiocontrast agent induced kidney injury in a mammal are disclosed, the methods comprising administering to the mammal a first effective amount of a chalcogenide composition prior to administering a radiocontrast agent to the mammal.
US20120329712 Induction of Differential Stress Resistance and Uses Thereof This invention relates to methods of inducing differential stress resistance in a subject with cancer by starving the subject for a short term, administering a cell growth inhibitor to the subject, or reducing the caloric or glucose intake by the subject. The induced differential stress resistance results in improved resistance to cytotoxicity in normal cells, which, in turn, reduces cytotoxic side-effects due to chemotherapy, as well as improved effectiveness of chemotherapeutic agents.
CN101983635A Juice for treating glaucoma The invention discloses a preparation method for treating glaucoma. The preparation method is realized by the following technical scheme: placing white chrysanthemum, safflower and Szechwan gentian into a drying oven for drying, heating the materials for 10-20min at the temperature of 90-150 DEG C, smashing corn kernels of different sizes by calamines, placing halite, alum, the white chrysanthemum, the safflower, the Szechwan gentian and the calamines into a white steel pot together, adding well water in the proportion of 1:1, heating the mixture, stopping heating until the mixture is boiled for 20m, cooling the mixture, heating the mixture for twice again, filtering the mixture to remove slag, and packaging the slag-removed product to obtain the finished drug juice. The drug juice can improve the curative effect obviously.
WO2012164572A1 Substituted 4-arylthiazoles and process of preparation thereof The present invention relates to novel substituted 4-arylthiazoles, their preparation, and to their use as therapeutic agents, particularly in the prevention or treatment of tuberculosis. The resent invention articularl relates to com ounds of formula A:
EP1453501B1 N- aryl-n'-arylcycloalkyl-urea derivatives as mch antagonists for the treatment of obesity The present invention discloses compounds of the formula I which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
WO2012030050A9 Pharmaceutical composition for prevention or treatment of degenerative neurological brain disorders The present invention relates to a pharmaceutical composition for the prevention or treatment of degenerative neurological brain disorders and, more specifically, relates to a pharmaceutical composition for the prevention or treatment of degenerative neurological brain disorders, such as Parkinson's disease, Alzheimer's dementia (senile dementia), stroke, Lou Gehrig's disease, Pick's disease, Creutzfeldt-Jakob disease, Huntington's disease, progressive supranuclear palsy, spinocerebellar degeneration, cerebellar atrophy, multiple sclerosis, post-traumatic stress disorder and amnesia, the composition containing a paraben compound as an active ingredient having effects that are useful in combating oxidation to remove active oxygen, suppressing cell-death, improving impaired movement, and enhancing declining memory.
US7700591 to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
WO2009038695A1 Method of treating gaucher disease Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.
CN1872063B Microspheres or composition in use for long acting injection of Nalmefene or its salt, and preparation method A microball for the long-acting injection to prevent and treating the recurrence of heroin addiction is proportionally prepared from nalmefene or its salt and biodegradable high-molecular medicinal auxiliary. Its composition is prepared from said microballs, suspending aid, scaffolding agent, lubricant and osmotic pressure regulator through proportional mixing and freeze-drying. Its release period can reach 20-40 days.
US20080193508 Local anti-infective agent for treatment of nail fungal infections A topical composition for treating nail fungal infections that utilizes an acidic antifungal agent with a molecular weight no greater than 170 Daltons in a formulation having a pH less than or equal to the pKa of the acidic antifungal agent plus one. Possible antifungal agents include omadine, octanoic acid, sorbic acid, hexanoic acid, and benzoic acid. The antifungal agent can be combined with a delivery system such as a lacquer, a gel, a patch, or a hydrating system. A second therapeutic agent such as a 5-fluorocystine or terbinafine can be included.
US7309706 Method for the treatment of diseases requiring inhibition or a reduction in the activity of pH value-regulating bicarbonate transporter proteins The use of selective imidazoline receptor agonists, such as moxonidine, rilmenidine, LNP-509, S-23515, PMS-812, PMS-847 and BU-98008, and their physiologically compatible acid addition salts in pharmaceutical preparations for the treatment and/or inhibition of functional disorders and/or diseases in larger mammals or humans which require inhibition or reduction of the activity of proteins which regulate the intracellular pH value and which belong to the superfamily of bicarbonate transporters, in particular the treatment or inhibition of clinical conditions of bones which are caused by an undesirable amount of bone resorption, such as osteoporosis; of diseases of the gastrointestinal tract, such as gastric ulcers; and of neuronal and/or neuropsychiatric diseases associated with a pathologically altered (especially increased) neuronal activity, such as depression, Alzheimer's disease, eating disorders and schizophrenia.
CN101417081A Quality control method of Longfengbao capsule The invention relates to a quality test method for Long Feng Bao capsule, which comprises identifications of borneol and tree peony bark. The quality test method is characterized in that the utilization of thin layer chromatography is added. With assaying methods of identifying herba epimedii qualitatively by positive control of icariin and measuring astragaloside by thin layer chromatography scanning, the invention improves the specificity of the qualitative identification method of the quality test method for Long Feng Bao capsule and simultaneously provides a quantitative test method for astagaloside to control the product quality more effectively, thereby insuring the safety and validity of the medication of human bodies. The quality test method can also be adopted as quality test methods for other oral preparations of the same prescription (crude drug of the same proportion), curative oral solutions, tablets and granules.
CN102429905A Medicinal composition containing tetrahydropalmatine and imperatorin The invention discloses a medicinal composition containing tetrahydropalmatine and imperatorin and application. The medicinal composition is prepared into various pharmaceutically acceptable solid oral formulations, such as granules, powder, tablets, pills and capsules, from the tetrahydropalmatine and the imperatorin in a weight ratio of (1-8):(1-5). Pharmacological tests show that the composition has the effects of suppressing pain and discomforts, including headache, migraine, stomachache, neuralgia, lumbago and menstrual pain; and the composition can be used for treating the pains.
CN103145762A Divalent-platinum complex containing sterically-hindered aryl group and preparation method and application thereof The invention discloses an antitumor platinum (II) complex which takes a chiral trans-1, 2-cyclohexanediamine derivative containing a sterically-hindered aryl group as a ligand. The antitumor platinum (II) complex has a structural formula I or II, wherein in the structural formula I, X is H, OCH3 or F and is in the ortho, meta or para position of N-methylene in a benzene ring, in the structural formula II, X is H, OCH3 or F and is in the ortho, meta or para position of N-methylene in a benzene ring, Z is oxalate, malonate, 1, 1-cyclobutyl diacid radical or 3-hydroxy-1, 1-cyclobutyl diacid radical. Two chiral carbon atoms in the trans-1, 2-cyclohexanediamine group have the same three-dimensional configuration and are both in the R or S configuration. The invention also discloses a preparation method of the platinum complex and an application of the platinum complex to the preparation of an anti-tumor medicament.
US20120142689 Serotonin reuptake inhibitors In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
WO2008116809A1 Pharmaceutical compositions comprising a bisphosphonate and vitamin d Parenteral pharmaceutical compositions comprising vitamin D, or a bisphosphonate and vitamin D for treatment or prevention of diseases of abnormally increased bone turnover and/or vitamin D deficiency.
CN103006642A Application of alkyne methylene indole-2-one derivative The invention relates to the field of pharmaceutical chemistry, in particular relates to a medical use of a unitary E-type configuration 3-site alkyne methylene substituted indole-2-one compound, and a pharmaceutical composition containing such compounds, and especially application as a cholinesterase inhibitor. Pharmacological experiments show such a compound has good cholinesterase inhibition activity, and has favorable application prospects in the field of treating Alzheimer disease, schizophrenia, chronic brain damage, facial paralysis, hemiplegia and the like.
CN102198235A Medicament for treating intervertebral disk herniation The invention relates to a medicament for treating intervertebral disk herniation, prepared from the following raw materials in parts by weight: 9-15g of dangshen, 9-15g of raw radix astragali, 9-15g of spatholobus stem, 9-15g of mistletoe, 9-15g of dodder, 6-9g of psoralea fruit, 6-9g of ground beetle, 6-9g of stir-fried typha pollen, 3-6g of centipede, 3-9g of long-noded pit viper, 3-9g of scorpion, 9-30g of prepared rehmannia root, 3-9g of epimedium, 6-9g of cistanche, 3-9g of deerhorn glue, 3-9g of ass-hide glue, 3-9g of pyrite, 3-9g of chicken's gizzard-skin, 6-9g of medicated leaven and 9-15g of rice-grain sprout. The medicament provided by the invention has no toxic side effects, quick effect taking speed, low recurrence rate and low treatment cost.
CN103599100A Application of Manzamenone O in drug for treating alzheimer disease The invention discloses novel application of Manzamenone O for the first time. Manzamenone O has acetylcholin esterase inhibitory activity and nerve cell protection function and serves as a multi-effect target compound to be used for preparing a drug for treating alzheimer disease. Manzamenone O has a brand new type of skeleton, has high inhibitory activity for acetylcholin esterase as well as outstanding substantial characteristics, and also shows a remarkable progress on prevention and treatment of alzheimer disease.
US20090163441 Hyaluronic Acid Binary Mixtures and Therapeutic Use Thereof The present invention is related to hyaluronic acid compositions consisting in a binary mixtures of hyaluronic acid samples having mainly different weight-average molecular weight and then different rheological properties in aqueous solution. The resulting compositions have demonstrated peculiar rheological behaviour with a balance between viscosity and viscoelasticity. Accordingly, these compositions of hyaluronic acid are useful for treatment of joint diseases by intra-articular administration or extra-articular application in soft tissue disorders.
US20110015395 Pyrazole compounds with inhibitory activity against ros kinase Disclosed herein are novel pyrazole compounds, pharmaceutically acceptable salts thereof, a method for preparing the same, and uses thereof as anticancer agents.
US20120316234 Anthraquinone -based compound, the synthesis processes and the application thereof The present invention is related to an anthraquinone-based compound represented by compound (I) wherein the R1, R2, R3, R4, R5 or R6 is selected by the group of H, amide, amino-amide, acyl, chloroacetamide, chloropropionamido, a substituted chloroacetamide and a substituted chloropropionamido. The present invention is also related to the method of producing the anthraquinone-based compound and the application thereof.
CA2266393C Aqueous antimicrobial liquid cleaning formulation comprising a polymeric deposition aid An aqueous, antimicrobial liquid cleaning formulation including: 1) a polymeric deposition aid composed of a mixture of liquid, hydroxyl-terminated urethane polymers in polyethylene glycol; 2) a phenol derivative antimicrobial agent; and 3) a surfactant system comprising predominantly nonionic surfactants, amphoteric surfactants or combinations thereof such that the liquid cleaning formulation provides at least about 10 percent greater antimicrobial activity than the same formulation without the polymeric deposition aid.
US20110207732 Azaindole derivatives Compounds of the formula (I), in which X1, X2, X3, X4, R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
CN1565456A Cefepime compound antibacterial drugs The invention discloses a cefepime antibacterial drug comprising cefepime and beta-lactam enzyme inhibitor by the ratio by weight of 1:2 to 1:0.1, wherein the cefepime is cefepime inner salt, or cefepime hydrochlorate, or cefepime hydrochlorate hydrate, or one of the former medicaments with added adjunct (L-arginine, or sodium carbonate, or sodium hydrogen carbonate, the beta-lactam enzyme inhibitor can be Tazobactam, or clavulanic acid, or tapazole or their derivatives.
US6884804 Inhibitors of Src and other protein kinases The present invention provides compounds of formula I: wherein A is N or CR, and G, R1, R2 and R3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of Src mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
CN102327215A Medecamycin nanoemulsion antibacterial drug and preparation method thereof The invention discloses a medecamycin nanoemulsion antibacterial drug. The nanoemulsion antibacterial drug has the particle size of 1-100 nm, and is prepared from the following raw materials in percentage by mass: 0.4-25.0% of ethyl acetate, 20.0-84.0% of Tween-80, 8.0-34.0% of ethanol, 0.01-10.0% of medecamycin and the balance of distilled water, wherein the sum of the mass percentages of the raw materials is 100%. The medecamycin nanoemulsion greatly improves the antibacterial and sterilization effects of medecamycin, enhances the dissolubility, safety and bioavailability, and is a high-efficiency antibacterial nanoscale drug preparation which is convenient to use and has a wide administration range; and the production process of the drug is simple, and mass production can be achieved without need of special instruments.
US20050150489 Dispensing medicaments based on rates of medicament action A method of dispensing a medicament. A treatment plan having at least two rates of action for a medicament may be provided. A droplet characteristic corresponding to each rate of action may be selected. Medicament droplets having each droplet characteristic may be ejected into a mucosal tract according to the treatment plan, thereby allowing the medicament to act at two or more rates.
US7754876 Method for purification of lactose The present invention relates to improved methods of purification of sugars and in particular to a method of preparing lactose. A low purity lactose source such as whey is subjected to a first demineralization step involving either ion-exchange or the addition of divalent metal cations, followed by a second demineralization step where alcohol is added. The invention also relates to lactose produced by this method and products comprising lactose produced by this method.
WO2014040373A1 Pi3k and/or mtor inhibitor Provided are a class of compounds of general formula (I), pharmaceutically acceptable salts, stereoisomers and solvates thereof, as well as a preparation method of the compounds and pharmaceutical compositions containing the compounds of general formula (I). Also provided are the uses of the compounds in the preparation of drugs for treating and/or preventing proliferative diseases.
US20090317470 Oramucosal Pharmaceutical Dosage Form This invention relates to an oramucosal pharmaceutical dosage form in the form of a wafer. The wafer comprises a porous, hydroscopic, muco-adhesive polymeric matrix with at least one desired pharmaceutically active compound added thereto. The polymer is selected from a number of polymers having different dissolution rates and, in use when taken orally, the matrix adheres to an oramucosal surface to dissolve over a predetermined period of time to release the pharmaceutically active compound. The invention also extends to a method of manufacturing an oramucosal pharmaceutical dosage form in the form of a wafer which involves freeze drying or lyophilisation.
US7384920 Using a stilbene compound modified with hydroxy or alkoxy groups; antidiabetic agents; viricides This invention relates to a new use of stilbene derivatives or pharmaceutically acceptable salts thereof, especially in the manufacture of medicament for the prevention and treatment of diabetes or retrovirus associated diseases.
US20120214769 Novel Antagonists of the Glucagon Receptor The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
US20100233172 Methods of inhibiting quiescent tumor proliferation Improved compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders, and methods of screening to identify compounds for such treatments.
CN102600118A Application and preparation method of sibutramine in preparation of information therapeutic drug and novel drug prepared by preparation method The invention discloses application and a preparation method of sibutramine in preparation of an information therapeutic drug and a novel drug prepared by the preparation method. The information therapeutic drug is characterized in that the drug does not contact a human body directly during treatment, any substance ingredient of the drug can not be consumed, only drug information is utilized for physical treatment, but the chemical treatment effect can be achieved, a treatment window is enlarged by more than 1000 times, and the side effects of chemical treatment are avoided. After sibutramine is used as the information therapeutic drug, the contents of active ingredients are not changed, and sibutramine can also be used as a conventional preparation in the chemical treatment for secondary effective use.
EP0786990B1 Use of astaxanthin for retarding and ameliorating eye damage A method of retarding and ameliorating eye diseases and injuries is disclosed. The method comprises administering astaxanthin in a therapeutically-effective amount to prevent, retard or treat eye and central nervous system diseases or injuries, such as age-related macular degeneration and other central nervous system degenerative diseases, photic injury, ischemic diseases, and inflammatory diseases.
CN102366398A Multifunctional eye drops The invention discloses multifunctional eye drops, which adopt calcium heparin as an active component and chloramphenicol eye drops as a diluent. Specifically, 5-10 parts by mass of calcium heparin are added into 100 parts by mass of chloramphenicol eye drops, and 5-10 parts by mass of ethylparaben and 1-3 parts by mass of sodium chloride are added into the solution. Application of the multifunctional eye drops of the invention can relieve itching of eyes with a short time, eliminate eyeball hyperemia, and has no other toxic and side effect. Ethylparaben, sodium chloride and isoproterenol are added into the eye drops of the invention, and combination of the formula and chloramphenicol eye drops can relax ciliary muscles and has no influence on eye mydriasis, and has special effects on treating pseudomyopia and controlling the increase of myopia degree.
CN1961868A A rapidly disintegrating tablet of acid sensitive drug The invention relates to a drug compound, as one quick release tablet with acid sensitive active component as acid sensitive proton pump restrain agent, wherein said tablet can protect the active component in pH condition of mouth, and it uses fluid bed method to pack the active component to obtain the packed particles; then adds acid pH adjuster which can neutralize the pH condition of mouth, to avoid pack player being dissolved in mouth.
EP1042316B1 Indole derivatives useful a.o. for the treatment of osteoporosis A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: A represents an optionally substituted aryl group or an optionally substituted heterocyclyl group; Ra represents -CO-NRsRt wherein Rs and Rt each independently represents hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heterocyclyl or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclyl group; R1 and R2 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R1 and R2 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R3 represents hydrogen, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or alkylsulphonyl and arylsulphonyl; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of such a compound or composition in medicine.
CN102552909A Composition for treating proteinuria and preparation method for composition The invention relates to the field of medicine, and discloses a composition for treating proteinuria and a preparation method for the composition. The proteinuria can be effectively reduced by the composition using agonists of metabotropic glutamate receptors 1 and 5 as active ingredients. Preferably, (s)3,5-dihydroxyphenylglycine ((s)3,5-DHPG) in the agonists of the metabotropic glutamate receptors 1 and 5 can be used.
WO2007059421A3 Polymorphs of 5-cyclopropyl-2-(4-fluorophenyl)-6-[(2-hydroxyethyl)(methylsulfonyl) amino]-n-methyl-1-benzofuran-3-carboxamide and methods of making the same Substantially pure polymorphic forms of 5-cycloproρyl-2-(4- fluorophenyl)-6-[(2-hydroxyethyl)(methylsulfonyl)amino]-N-methyl-l- benzofuran-3-carboxamide are produced by recrystallization in an organic solvent.
EP1972339A1 Haemostatic Compositions The invention relates to a composition comprising: (a) one or more aminoacids selected from glycine, proline and hydroxyproline; (b) a source of calcium ions; and (c) water. The invention also extends to a dry composition comprising the aforementioned components (a) and (b). The compositions of the invention are useful for arresting bleeding of humans and other animals, in particular for accelerating haemostasis at the site of incisions made during surgical procedures.
CN103191057A Aqueous suspension injection of ceftiofur, and preparation method thereof The invention provides an aqueous suspension injection of ceftiofur. The aqueous suspension injection comprises 5-20% W/V of a ceftiofur micronized raw material, 8-15% W/V of a water-soluble excipient, 5-25% W/V of a suspending agent, 0.1-0.5% W/V of a suspending aid, and balance of injection water. Compared with traditional ceftiofur oily suspension liquids, no organic solvent is added into the ceftiofur aqueous suspension injection. The ceftiofur aqueous suspension injection is substantially a pure water solution. Therefore, problems of high viscosity and inconvenient application of current ceftiofur oily suspension liquids in market are solved.
US7914778 Methods of treatment using IL-16 antagonist peptides The present invention has found that a series of peptides having sequences that substantially correspond to specific regions of the C-terminus of IL-16 can inhibit the activity of IL-16. The present invention has demonstrated that such IL-16-inhibiting peptides can be as short as 4 amino acids in length. Based on these discoveries, the present invention provides IL-16 antagonist peptides and the use thereof for the treatment of IL-16 mediated disorders such as certain inflammatory diseases.
WO2009054439A1 Pai-1 production inhibitor Disclosed is a compound represented by the general formula (I) below, which has PAI-1 production inhibitory activity. (I) (In the formula, R1 represents, for example, a hydrogen atom or a 4-(morpholinyl)carbonyl group; ring D represents, for example, a benzene ring or a substituted benzene ring; phenyl group E has a substituent such as a halogen atom, a halogenated alkyl group, an alkyl group, an halogenated alkoxy group or an alkoxy group.)
CA2279184C Pharmaceutical compositions containing ibuprofen and domperidone for the treatment of migraine Migraine is treated by administering to the patient a pharmaceutical composition containing a therapeutically effective amount of ibuprofen or a salt thereof and a therapeutically effective amount of domperidone or a salt thereof.
WO2013057205A1 Diazabicyclo- and diazaspiro-alkane derivatives as phosphodiesterase-5 inhibitors The present invention describes novel PDE5 inhibitors that contain a diazabicyclo- or diazaspiro-alkane radical. These diazabicyclo- and diazaspiro-alkane radicals can be regarded as conformationally fixed piperazine analogs, where some of these novel compounds have improved properties compared to vardenafil and sildenafil, for example.
CN1923248A Five-poison medicine for treating tumor The invention relates to a medicinal composition for treating tumor which comprises croton, seed of nuxvomica, ginseng, oldenlandia, centipede, boneol, white alum, buthus martensi karsch, bee honey and rapeseed oil, and the preparing process consists of making powders, mixing, charging rapeseed oil and frying, and charging bee honey to obtain grease form.
US8647826 Nucleic acid and corresponding protein entitled 125P5C8 useful in treatment and detection of cancer A novel gene (designated 125P5C8) and its encoded protein, and variants thereof, are described wherein 125P5C8 exhibits tissue specific expression in normal adult tissue, and is aberrantly expressed in the cancers listed in Table I. Consequently, 125P5C8 provides a diagnostic, prognostic, prophylactic and/or therapeutic target for cancer. The 125P5C8 gene or fragment thereof, or its encoded protein, or variants thereof, or a fragment thereof, can be used to elicit a humoral or cellular immune response; antibodies or T cells reactive with 125P5C8 can be used in active or passive immunization.
CN101360741A Substituted 5-heteroaryl-1-phenyl-pyrazole cannabinoid modulators This invention relates to acannabinoid modulator compound of formula (I) for used in cannabinoid receptor mediated syndrome.
CN1583043A Duyiwei extract and its preparation and use An extract of lamiophlomis herb is disclosed, which has antalgic, inflammation-relieving and blood-circulating functions. Its preparing process and application are also disclosed.
CN102204871A Composition for weight loss The invention relates to a composition for weight loss. The composition is formed by uniformly mixing a mast cell stabilizer, such as sodium cromoglycate powder and the like, and sesamin powder extracted from sesames, in the proportion of 1: (1-100), wherein the content of sodium cromoglycate in the sodium cromoglycate powder serving as the mast cell stabilizer is more than 98 percent; and the content of sesamin in the sesamin powder is more than 50 percent. The composition is mixed with a makeup preparation or an excipient of a medicament to prepare an external preparation for skin, such as a cream, an emulsion, a gel, a lamination film, a subcutaneous injection and the like. Pharmacological experiments show that the composition has the effects of reducing weight, fat, the number and the volume of fat cells, blood sugar and blood fat. Local stimulation experiments show that the composition is safely used. Results of tests on obese people show that the composition has the functions of reducing weight and eliminating fat, is safely used and has no side effect.
US20110105605 Method of preparing a latanoprost ophthalmic solution and the resulting solution A method of solubilizing an analog active agent of the prostaglandin F2α, such as latanoprost, is described and a method of preparing an ophthalmic solution of the solubilized latanoprost for the treatment of distinct ocular ailments. This invention also refers to an ophthalmic aqueous solution resulting from the aforementioned method, which is characterized by its chemical stability at room temperature, its safety, and innocuousness and efficiency in the treatment of the patient. The new ophthalmic aqueous solution is distinguished because its pharmaceutical value is found in the handling of a vehicle of easy access that not only permits the solubility of latanoprost, but also promotes its chemical stability and a greater tolerance of the patient with its ophthalmic application for the treatment of the patient's ailment.
US20110190393 Novel and efficient method for the synthesis of an amino acid The present invention relates to a novel process for the preparation of γ-amino acids, such as (±)-3-(aminomethyl)-5-methyl-hexanoic acid (1), which is a key intermediate in the preparation of the potent anticonvulsant pregabalin, (S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid (2), and its analogues.
US20120065199 Substituted quinolines for use as vegf inhibitors A compound of formula (I) as well as pharmaceutically acceptable salts thereof and pharmaceutical compositions including a therapeutically effective amount of the compounds. The compound is useful in treatment of cancer, diabetic retinopathy, age-related macular degeneration, inflammation, stroke, ischemic myocardium, atherosclerosis, macular edema and psoriasis.
US8066975 Psoriasis or seborrheic dermatitis; mixture of clobetasol propionate, an anionic surfactant (sodium lauryl ether sulfate), an amphoteric surfactant ( cocamidopropyl betaines); a propenetrating agent chosen from ethanol, isopropanol, propylene glycol and ethoxydiglycol; foam with good compactnes; shampoo The invention concerns a foaming composition for washing and treating hair and/or scalp essentially characterized in that it contains in an aqueous medium: at least an active principle selected among corticoids and retinoids; at least an anionic surfactant; at least an amphoteric surfactant; and a pro-penetrating agent.
WO2009071519A1 Oxadiazole derivatives and their use as nicotinic acetylcholine receptor modulators The present invention relates to novel oxadiazole derivatives as nAChR agonists having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of neurological, psychiatric disorders and gastrointestinal disorders.
WO2006043594A1 1,5-diheterocycle-1h-triazole derivative A compound represented by the general formula (I): (wherein Ar1, Ar2, R1, and R2 each represents a substituent), a salt thereof, or a solvate of either; and a medicine containing the compound, salt, or solvate. The medicine is a potent platelet aggregation inhibitor which inhibits neither COX-1 nor COX-2.
US20070238767 e.g. 4,5-Dihydro-2-(2,4-dihydroxyphenyl)-thiazole-4(S)-carboxylic acid; ferrochelatase; thalassemia, anemia; diagnosing and treating pathological conditions associated with excess of trivalent metals (such as Fe, Al and Cr) The present invention relates to novel thiazoline acids and derivatives thereof useful as chelators of trivalent metals in therapeutic applications. For example, the thiazoline acid derivatives are useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.
US20120128738 Theobromine for the Treatment of Cough The present invention is theobromine as an active agent to be delivered via the inhaled route, for the treatment of cough.
US20120295898 Antiviral Therapy The present invention relates to combinations of compounds comprising HIV integrase inhibitors and other therapeutic agents. Such combinations are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
EP1492876B1 Cationic amphiphiles for intracellular delivery of therapeutic molecules, composition, process and use thereof The present invention provides novel cationic amphiphiles (1) capable of facilitating transport of biologically active molecules into cells wherein the said amphiphiles contain cyclic head group having polar functional groups and pharmaceutical composition useful for delivering biologically active therapeutic molecules into body cells.(1)
CN103599137A Health food containing plurality of trace nutrient elements The invention provides a healthcare food containing a plurality of trace nutrient elements, and belongs to the technical field of trace nutrient element healthcare food. The healthcare food is composed of twenty eight kinds of materials, namely calcium, magnesium, zinc, iron, selenium, manganese, copper, chromium, cobalt, molybdenum, vitamin A, vitamin C, vitamin E, vitamin D, vitamin B1, vitamin B2, vitamin B6, vitamin B12, nicotinamide, pantothenic acid, biotin, folic acid, resveratrol, procyanidine, astaxanthin, lycopene, xanthophylls, and zeaxanthine. The healthcare food organically compounds a plurality of essential mineral substances, vitamins, and antioxidant plant extracts together and presses the materials into tables or capsules. The elements in the healthcare food cooperates with each other to generate a balanced and synergetic effect; the supply amount of biological elements is sufficient; the element ratio is balanced and harmonious, is totally in a safe range of diet recommended amount provided by Chinese Nutrition Society, and the health food provides an enough amount of nutrient elements for body physiological activities and body functions of preventing diseases and removing toxicity on the basis of safety.
US20110251217 Substituted purinyl-pyrazol derivatives and their use as potassium channel modulators This invention relates to novel substituted purinyl-pyrazol derivatives of formula (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
WO2011060492A1 Combination for treating metabolic disorders Methods of treating, preventing, reducing or mitigating inflammation and/or oxidative stress, enhancing zinc uptake, regulating the lipid profile to produce a favourable lipoprotein / lipid profile and/or improving glycaemic control in an individual, comprising administering a therapeutically effective amount of a combination of zinc and an omega-3 fatty acid to the individual.
US20110177031 Eicosapentaenoic Acid-Producing Microorganisms, Fatty Acid Compositions, and Methods of Making and Uses Thereof The present invention is directed to isolated microorganisms as well as strains and mutants thereof, biomasses, microbial oils, compositions, and cultures; methods of producing the microbial oils, biomasses, and mutants; and methods of using the isolated microorganisms, biomasses, and microbial oils.
CA2753847A1 Methods for treating ocular inflammatory diseases A method of treating blepharitis includes administering to the affected eye of a subject an effective amount of an active ingredient in an ophthalmically acceptable vehicle for a sufficient period of time to treat blepharitis. The active ingredient consists essentially of a glucocorticoid in an ophthalmically acceptable vehicle that includes an aqueous polymer suspension that when mixed with tear fluid provides a sustained release of said active ingredient. The aqueous polymer suspension includes a carboxyl-containing polymer having less than about 5% by weight cross-linking agent and has a viscosity in a range from about 1,000 to about 30,000 centipoises. A kit includes: (a) a composition comprising about 0.1% by weight dexamethasone in this ophthalmically acceptable vehicle and (b) instructions for using the composition of (a) for the treatment of blepharitis.
US20130224320 Process to improve feed efficiency and carcass characteristics of animals This invention relates to a process to improve the feed efficiency and carcass characteristics of an animal. The process of this invention can be used to decrease the cost of animal diets, to improve performance of animals and to improve the percentage of carcass in animals.
WO2012028106A1 Deuterium-enriched heterocyclic compounds as kinase inhibitors The present invention provides deuterium-enriched heteroaryl-containing urea compounds (I) and use of the same for treating conditions mediated by protein kinase such as
US20120177626 Hdl comprising a therapeutic agent and use in therapy The present invention provides an HDL comprising an agent selected from the group consisting of antiproteases, antixoxidants, antimitotics, anti-apoptotic agents and agents involved in the iron metabolism for use as a medicament.
US20100285029 Treatment of fungal infections with polyene or beta glucan synthase inhibitor anti-fungals combined with anti-hsp90 antibodies The present invention relates to novel compositions and preparations that are effective antifungal agents, and a novel antibody which can be incorporated into the compositions and preparations.
CN102178767A Carsickness plaster and preparation process thereof The invention discloses a carsickness plaster and a preparation process thereof. The plaster is composed of a backing layer, a glue layer, an anti-sticking layer. The glue layer comprises, on a weight basis, 85%-95% of polymer glue, 1%-5% of peppermint oil, 1%-5% of eucalyptus oil, 1%-5% of lemon oil, and 0.5%-1.5% of methyl salicylate. Firstly, the polymer glue is added into a glue boiler for heating and melting; then the other materials of the components are added and are stirred for uniform dispersion so as to obtain the glue layer; finally, the backing layer, the anti-sticking layer and the glue layer are loaded on a plaster coating machine group for coating and cutting to obtain the carsickness plaster of the invention. The carsickness plaster of the invention is applied at the retroauricular hairless region, can prevent vertigo and vomit caused by carsickness, seasickness, airsickness, has the effect of refreshment, has high safety, no toxic side effects, and can cool continuously for about six hours.
CA2480065C Injectable veterinary composition for small animals An injectable aqueous composition for veterinary use containing a non-steroidal anti-inflammatory compound in an amount of from about 0.25 to 30% (w/v) together with a physiologically acceptable oxygenated polymeric surfactant in an amount of from about 0.5 to 20% (w/v).
CN101584697A 6H-thiochromeno[3, 4-e][1, 2, 4]triazolo[1, 5-a] pyrimidine compounds with anticancer activity The invention discloses a sulfur-nitrogen contained four-ring heterocyclic compound, particularly a 6H-thiochromeno[3, 4-e][1, 2, 4]triazolo[1, 5-a] pyrimidine compound with anticancer activities. Aiming at the current research and development situations of few anticancer medicines with large toxicity in the prior art, the 6H-thiochromeno[3, 4-e][1,2,4]triazolo[1, 5-a] pyrimidine compound anticancer experiment is made, and an RPMI Medium 1640 is used as a cell culture medium and a detecting method which is an MTT method is adopted in the experiment. An experimental result indicates that the compound has high anticancer activities in vitro and can be used as the anticancer medicine.
EP1495141A2 Hiv therapeutic The present invention provides siRNA methods and composi tions for inhibiting HIV and/or replication, as well as systems for identifying effective siRNAs for inhibiting HIV and systems for studying HIV infective mechanisms. The invention also provides methods and compositions for inhibiting infection, pathogenecityand/or replication of an infectious agent; for example, by using siRNAs to inhibit host cell gene expression.
WO2008018427A1 Aminophosphoric acid ester derivative and s1p receptor modulator containing the same as active ingredient Disclosed is an aminophosphoric acid ester derivative having excellent sphingosine-1-phosphate (S1P) receptor modulating activity. Specifically disclosed is an aminophosphoric acid ester derivative represented by the general formula (1) below, which is a highly safe compound having a strong S1P receptor modulating activity.
CN102884064A Processes for the preparation of S1P1 receptor modulators and crystalline forms thereof The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
WO2008110080A1 Medical composition containing cyclodextrin inclusion compound of cefixime and its preparation method A medical composition containing the cyclodextrin inclusion compound of cefixime and its preparing method. Its basic components comprise a) cefixime, and b) a pharmaceutically acceptable cyclodextrin; said cyclodextrin is one or more components chosen from β-cyclodextrin, sulfobutyl ether-β-cyclodextrin,hydroxypropyl-β-cyclodextrin,hydroxypropyl-sulfobutyl ether-β-cyclodextrin.
CN1823777A Nicergoline soft capsule and its preparation method A soft capsule of nicergoline is prepared from nicergoline, diluent, cosolvent, suspending aid, surfactant and crystallizing inhibitor through mixing.
EP1519722A1 Glycoloyl-substituted oxazolidinone-derivatives as antibacterial agents The present invention describes difluororthioacetamide oxazolidinones_of formula I with a glycoloylpiperazine substituent as novel antibacterial agents, and antimicrobial combination therapies for combatting infective diseases caused by gram-positive and gram-negative bacteria.
WO2013132376A1 Macrocyclic derivatives for the treatment of proliferative diseases The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.
WO2005037816A1 Use of 8-prenylnaringenin for hormone replacement therapy The invention provides a production method for the phytoestrogen 8-Prenylnaringenin, the preparation produced by this method and the use of 8-Prenylnaringenin for the production of a medicament for the prevention and treatment of hormone-dependent osteoporosis and of peri- and postmenopausal symptoms in women.
US20120225911 Replenishing body stores of fat-soluble vitamins A, and D eradicate chronic viral infection The invention relates to beta-carotene and its' related analogues, zinc, vitamin D3, and niacin to enhance the performance of the innate and adaptive immune system. Beta-carotene and its' related analogues are converted to retinoic acid that activates retinoic acid receptors, retinoid X receptors and niacin activates the retinoid X receptors and peroxisome-proliferator-activated receptors to increase transcription activities or high density lipids(HDL). Zinc is required for transport of retinol and its conversion to retinal. Vitamin D activates transcription in activated immune cells. The overall effect of the composition is to improve the response of the immune system to effectively remove viral, bacterial, and other invading pathogens.
EP1392255B1 Nanoparticles made of protein with coupled apolipoprotein e for penetration of the blood-brain barrier and methods for the production thereof The invention relates to nanoparticles for penetration of the blood-brain barrier, characterized in that they consist of a hydrophilic protein or a combination of hydrophilic proteins, preferably serum albumen, most preferably of human origin, which is coupled to apolipoprotein B. the invention also relates to methods for the production of said nanoparticles.
CN103372018A Application of Chukrasone A in preparation of medicines for increasing blood platelets The invention relates to a new application of a Chukrasone A compound in the pharmaceutical field, and particularly relates to an application of the Chukrasone A in the preparation of medicines for increasing blood platelets. The application of the Chukrasone A in the preparation of the medicines for treating the reduction of blood platelets is disclosed for the first time. As the skeleton type of the Chukrasone A belongs to a bran-new skeleton type and the Chukrasone A has unexpected strong inhibitory activity on the reduction of the blood platelets, the possibility that other compounds provide revelation does not exist. The Chukrasone A has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for preventing and treating the reduction of the blood platelets.
US20120108533 Novel phosphate modified nucleosides useful as substrates for polymerases and as antiviral agents This invention provides phosphate-modified nucleosides represented by the structural formula: wherein W is O or S, and wherein B, R1; R3 and R2. are s defined herein. These compounds are useful as substrates for DNA/RNA polymerases, and as anti-viral agents in particular against HIV-1.
CA2842777A1 Pharmaceutical compositions comprising sulbactam and beta-lactamase inhibitor Pharmaceutical compositions and methods for treating or preventing bacterial infections are disclosed. The pharmaceutical compositions typically comprise pharmaceutically effective amount of: (a) sulbactam or a pharmaceutically acceptable salt thereof, and (b) at least one beta-lactamase inhibitor or a pharmaceutically acceptable salt thereof, with the provision that the beta-lactamase inhibitor is not sulbactam.
CN101805325A Novel lignan compound and application thereof The invention belongs to the field of the chemical technology for natural products, and relates to a novel lignan compound, which is used as an inhibitor of various protein tyrosine phosphatases (PTPs), in particular protein tyrosine phosphatase-1B (PTP-1B). The novel lignan compound provided by the invention has a structural formula as shown below, wherein R is hydroxyl, amino, alkoxy or amido, the alkoxy is propoxy, ethoxy, propoxyl or isopropoxy; the amido is primary amido or secondary amido with the alkyl being C1-C4 alkyl; and the absolute configuration of two chiral carbons is of R type or S type. The novel lignan compound of the invention can be applied in preparation of (PTP-1B) inhibition drugs.
WO2013074906A1 Compositions for controlling food intake and uses therefor The present invention is directed to a combination treatment for: individuals who meet the definition of food addiction; individuals that are overweight or obese (e.g., a BMI > 25); individuals that have a binge eating disorder; or individuals who engage in a binge eating behavior. In particular embodiments, the combination therapy reduces the intake of fatty foods, sugar rich foods, or foods that are both fatty and sugar-rich (e.g., such as fast foods).
US20050014793 Pyridinone derivatives for treatment of atherosclerosis Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis. Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
CN1650874A Preparation method of oligosaccharide kind health care product A health-care oligose food is prepared from oligochitose, oligoxylose and Vc through proportionally mixing, stirring and high-temp sterilizing. Its advantages are high effect and easy absorption.
CN103284970A Sarpogrelate hydrochloride sustained release preparation and preparation method thereof The invention relates to a sarpogrelate hydrochloride sustained release preparation and a preparation method thereof. The sarpogrelate hydrochloride sustained release preparation provided by the invention is invented for slowing down the release speed of a sarpogrelate hydrochloride medicine. The main components of the preparation provided by the invention can release medicines continuously in the gastrointestinal tract for over 24 hours.
US20120329754 Topical skin barrier A topical skin barrier for protecting and promoting healing of skin, and for providing comfort to a patient, comprises a semi-solid hydrocarbon and a water-absorbing compound. The topical skin barrier effectively adheres to skin, affords protection from moisture and waste, and provides transparency in use. Methods of in vitro evaluation are for (i) a composition's protection from moisture and waste, and (ii) a composition's adhesion to skin.
US20110028390 Pyrazolospiroketone Acetyl-CoA Carboxylase Inhibitors The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of acetyl-CoA carboxylase enzyme(s) in an animal.
US20100317672 Monomaleate Monohydrate Salt of a 5HT1A Receptor Antagonist The present invention relates to a monomaleate monohydrate salt of 7-methyl-6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4,5-dihydroimidazo[1,5-a]quinoline-3-carboxamide, uses of the salt as a medicament in the treatment of sexual dysfunction and pharmaceutical compositions and dosage forms comprising the salt.
US7049084 Neuroblastoma cell lines expressing the α2δ subunit of calcium channels and methods therefore The present invention provides methods for identifying test substances that bind to the α2δ subunit of a calcium channel.
WO2013192078A1 Synthetic pgpg analogs, methods of preparation and methods of use The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, and L are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating and preventing bacterial infections, and methods of identifying pGpG-binding domains in bacteria, using the compounds of Formula I.
EP2766002A2 R(+)-n-formyl-propargyl-aminoindan The subject invention provides R (+) -N-formyl-propargyl- aminoindan and a composition containing N-propargyl-1 (R) -aminoindan or a pharmaceutically acceptable salt thereof, and a compound of R (+) -N-formyl-propargyl-aminoindan.
US20080025984 Combination Therapy Comprising Cloretazine This invention provides a method for treating tumor in a subject comprising administering to the subject an effective amount of: (1) VNP40101M, or its equivalent; and (2) a nucleoside, or a nucleoside analog. This invention also provides a method for inhibiting tumor cell growth comprising contacting the tumor cell with effective amounts of: (1) VNP40101M, or its equivalent; and (2) a nucleoside, or a nucleoside analog. The present invention relates to the treatment of cancer, comprising administering to a subject in need thereof an effective amount of VNP40101M in combination with a nucleoside.
CN102743366A Paracetamol effervescent granule and identification method thereof The invention discloses a paracetamol effervescent granule. The paracetamol effervescent granule comprises, by weight, 2%-7% paracetamol, 5%-30% of effervescing agents, 65%-86% of filler, 0.6%-0.8% of flavoring agents and the balance bonding agents, the effervescing agents are composed of acid agents and alkaline agents, the mass ratio of the acid agents to the alkaline agents is 1:1.7, the acid agents are optionally two or three of citric acid, fumaric acid and tartaric acid, and the alkaline agents are sodium bicarbonate. The paracetamol effervescent granule is dissolved in water quickly to form clear and transparent solution great in taste, and is convenient to take, high in bioavailability, qualified in identification items and good in effervescence. The invention further discloses an identification method of the paracetamol effervescent granule, and the identification method is simple in operation and good in anti-interference effect.
CN101560230B Helicid extraction method The invention discloses a helicid extraction method, which aims at solving the problem of lower helicid extraction rate. The method comprises the following steps of: (1) crushing a helicid fruit into blocks, soaking and heating the helicid fruit until refluence, filtering residues and obtaining solution, and extracting the solution for three times repeatedly, combining, decompressing and concentrating the extraction solution; (2) heating the extraction solution obtained from the step (1) to 70-75 DEG C, adding a ZTC 1+1 II type clarifier B component, naturally cooling the solution to room temperature, centrifugally separating the solution to obtain clear solution, and concentrating the clear solution; (3) adding an organic solvent which is ethanol or acetone into the concentrated clear solution obtained from the step (2) and filtrating the solution to obtain filtrate; (4) adding medicinal activated carbon into the filtrate obtained from the step (3), heating the filtrate until refluence, decoloring and filtering the filtrate and collecting filtrate; (5) recycling the solvent from the filtrate obtained from the step (4) in normal pressure until 80 percent to 90 percent of the solvent is recycled, filtering at room temperature, washing with water, and drying to obtain the helicid. The method is mainly used for helicid extraction.
WO2013172682A1 Use of flavone compound for prevention or treatment of obesity The present invention relates to a pharmaceutical composition containing flavone compound as an active ingredient for treating obesity, and more specifically to a pharmaceutical composition for preventing or treating obesity and a dietary composition for preventing or reducing obesity containing 5,7-dimethoxyflavone or 5,7,4'-trimethoxyflavone. The compound according to the present invention inhibits adiopogenesis, and reduces expressions of the key transcription factors (SREBP1c and C/EBP) related to lipogenesis and of enzyme proteins (FAS and ACC) related to adiopogenesis, and thus is effective in preventing or treating obesity.
US20110166225 Oral liquid compositions of rhein or diacerein The invention relates to liquid pharmaceutical compositions for oral administration comprising rhein or diacerein, or salts or esters or prodrugs thereof and processes for preparing such compositions.
US20080293825 Hydroalcoholic antimicrobial composition with skin health benefits The invention pertains to an alcohol based antimicrobial skincare composition. The invention also pertains to an alcohol based antimicrobial skincare composition with skin health benefits including moisturization and skin barrier maintenance effects. The invention further pertains to an alcohol based antimicrobial skincare composition that is a stable emulsion that has a certain viscosity to it that provides containment, for example on a user's hands. Finally, the invention pertains to an alcohol based antimicrobial skincare composition that may be used in the healthcare industry, for example as a surgical scrub, healthcare personnel handwash, or patient pre-operative site preparation.
CN103316002A Application of compound in preparation of drug for treating breast cancer The invention discloses an application of a compound in preparation of a drug for treating breast cancer. Computer screening and in vitro and vivo activity test of the compound find that the compound namely 4-quinolyl (5-vinyl-1-azabicyclo [2.2.2]octane-2-yl)ketone has a strong inhibiting effect on ROCKI, has an obvious inhibiting effect on proliferation of breast cancer cell, has small compound cytotoxicity and a good development prospect, and is expected to be developed as a novel ROCK protein inhibitor, especially a ROCKI protein inhibitor. The compound is expected to be developed as a novel antitumor drug, especially a new drug for treating breast cancer.
EP1202744B1 PRODUCTION OF rhPBGD A method for production of rhPBGD in high scale and use of rhPBGD in a method for treatment or prophylaxis of disease caused by deficiency, in a subject, of an enzyme belonging to the heme biosynthetic pathway. The method comprising administering, to the subject, an effective amount of one or more catalyst which is said enzyme or an enzymatically equivalent part or analogue thereof prefreable in combination with a gene therapy of a mutation related to the catalyst. The disease is selected from the group consisting of acute intermittent porphyria (AIP), ALA deficiency porphyria (ADP), Porphyria cutanea tarda (PCT), Hereditary coproporphyria (HCP), Harderoporphyria (HDP), Variegata porphyria (VP), Congenital erythropoietic porphyria (CEP), Erythropoietic protoporphyria (EPP), and Hepatoerythropoietic porphyria (HEP). The catalyst is one or more enzymes selected from the group consisting of delta-aminolevulininic acid synthetase, delta-aminovulinic acid dehydratase (ALAD), porphobilinogen deaminase (PBGD), uroporphyrinogen III cosythetase, uroporphyrinogen decarboxylase, coproporphyrinogen oxidase, protoporphyrinogen oxidase, and ferrochelatase, or an enzymatically equivalent part or analogue therof. In addition the invention relates to the use of rhPBGD. The invention also relates to an expression plasmid pExp1-M2-BB (seq. ID No.1) and to use of a DNA fragment, the EcoR I - Hind III linear fragment (seq. ID No. 2), used for transformation in the hemC disruption strategy for production of rhPBGD expressed in E. coli..
WO2009064250A1 Bis-(sulfonylamino) derivatives in therapy 065 The invention provides compounds of formula wherein R1, R2 , R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
US7541329 Oil body associated protein compositions and methods of use thereof for reducing the risk of cardiovascular disease Compositions and methods for reducing hypercholesterolemia and, accordingly, the risk of cardiovascular disease, are provided. Such compositions may comprise isolated oil body associated proteins. Additionally provided are foodstuffs to which one or more oil body associated proteins have been added. The compositions employed in the invention may further comprise additive compounds, for example, a saponin, an isoflavone, a phospholipid, a carbohydrate substantially resistant to digestion, or a combination thereof. The methods and compositions of the invention may be used to lower cholesterol and other lipid levels in subjects to achieve a reduction in the risk of cardiovascular disease.
CA2793451A1 Aptamers to .beta.-ngf and their use in treating .beta.-ngf mediated diseases and disorders The present disclosure relates generally to the field of nucleic acids and, more particularly, to aptamers capable of binding to ß-NGF; pharmaceutical compositions comprising such ß-NGF aptamers; and methods of making and using the same.
CN1827170A Composition containing dihydropyridin type of calcium antagonists and fibrates medicine This invention is about a composition containing dihydropyridine calcium antagonist and phenoxy aryl acid drugs, and it belongs to medicine field. The composition contains medicine-dosage phenoxy aryl acid drugs or its salt that can be used in medicine, medicine-dosage dihydropyridine calcium antagonist or its salt, carrier or excipient that can be used in medicine. This invention also refers to the composition usage in preparing drugs those can be used to cure those who has afflicted or is prone to afflict with metabolism syndrome, and supplies an effective therapy scheme for metabolism syndrome.
CN103372022A Glucose health-care oral solution and preparation method The invention provides a glucose health-care oral solution which is researched aiming at hypoglycemia crowds and hypoglycemia patients caused by diabetes mellitus. The glucose health-care oral solution is an edible nutritional agent which is convenient to take, is easy to absorb, can rapidly have effects and is convenient to carry; injection crystallized glucose/oral crystallized glucose/edible-grade glucose syrup is used as a raw material and procedures of preparing materials, dissolving/diluting, de-coloring, primarily filtering and finely filtering are carried out to prepare a glucose health-care oral solution raw material; the glucose health-care oral solution raw material is packaged to prepare the glucose health-care oral solutions with the specifications of 15ml, 20ml and 25ml.
CN1857218A Slow released medicine containing antituberculotic The slow released implanting agent and injection containing antituberculotic are set or injected to local tuberculosis focus for maintaining the local effective medicine concentration while lowing the systemic toxicity. The slow released injection consists of slow released microsphere and solvent. The slow released microsphere includes antituberculotic selected from Cycloserine, Ofloxacin, Ciprofloxacin and Sparfloxacin and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow releasing supplementary material is selected from EVAc, PLA, PLGA, etc. The slow released implanting agent may be prepared with slow released microsphere. The present invention has obvious and unique treating effect on various kinds of intractable tuberculosis.
EP2701690A1 Method of treating lymphoma using pyridopyrimidinone inhibitors of pi3k/mtor The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of formula I.
WO2009118174A1 Substituted cyclohexyldiamines The invention relates to compounds which have an affinity for the μ opioid receptor and the ORL1 receptor, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.
WO2004089313A3 Novel olanzapine forms and related methods of treatment The invention provides novel soluble olanzapine forms. These forms include salts, co-crystals, and solvates of olanzapine. The invention also provides novel pharmaceutical compositions comprising these novel soluble forms and related methods of treatment. Compositions and methods of the invention of the invention are useful in the treatment of psychosis and functional bowel disorders.
EP1112005B2 Antioxidant composition comprising acetyl l-carnitine and alpha-lipoic acid A composition is disclosed which comprises as characterizing active ingredients acetyl L-carnitine and α-lipoic acid, for the prevention and/or therapeutic treatment of various alterations and pathological states induced by free radicals, that may take the form of a dietary supplement, dietetic support or of an actual medicine.
WO2009028580A1 Ebi3, dlx5, nptx1 and cdkn3 for target genes of lung cancer therapy and diagnosis The present invention relates to methods for treating or preventing lung cancer by administering a double-stranded molecule against one or more of EBI3, DLX5, NPTXl, CDKN3 or EF-I delta genes or compositions, vectors or cells containing such a double-stranded molecule. The present invention also features methods for diagnosing lung cancer, especially NSCLC or SCLC, using one or more over-expressed genes selected from among EBI3, DLX5, NPTXl, CDKN3 and/or EF-I delta. Also disclosed are methods of identifying compounds for treating and preventing lung cancer, using as an index their effect on the over-expression of one or more of EBI3, DLX5, CDKN3 and/or EF-I delta in the lung cancer, the cell proliferation function of one or more of EBI3, DLX5, NPTXl, CDKN3 and/or EF-I delta or the interaction between CDKN3 and VRS, EF-I beta, EF-I gamma and/or EF-I delta.
CN101708267A Medicament for treating frostbite and burn injuries The invention discloses a medicament for treating frostbite and burn injuries, which is prepared from the following raw materials in part by weight: 0.2 to 0.6 part of donkey-hide glue, 0.3 to 0.8 part of aloe, 0.5 to 2 parts of glacial acetic acid, 1 to 1.3 parts of chitin, 0.01 to 0.03 part of sodium chloride and 200 to 300 parts of distilled water. A preparation method for the medicament comprises the following steps of: taking the raw materials according to the formula, squeezing a juice of the aloe; after dissolving the chitin and the donkey-hide glue with a small amount of the distilled water respectively, adding the remaining distilled water with into solution of the chitin; and sequentially adding the glacial acetic acid, the aloe juice, the sodium chloride and the donkey-hide glue into the solution of the chitin under stirring to obtain gelling solution. The medicament is wide in adaptation diseases, has no toxic and side effects and no stimulation to skins and mucosae, is safe in use, is resistant to infections and relapse, and has a cure rate of 100 percent. The medicament is used without cleaning a wound surface to avoid pains to a patient caused by cleaning the wound surface and is in favor of reducing the infection to the wound part of the patient. The medicament can cure light and moderate skin burn injury wound surfaces in 10 to 20 days without scars left. The frostbite and the burn injuries will not relapse in the next year. In addition, the medicament has the advantages of simple operation and convenient use.
CN101138635B Fibrin glue vasodilation agent sustained-release long-acting composition The present invention relates to a long acting composition of the fibrin glue vasodilating agent with sustained release property, which comprises a vasodilating agent and a spasmolysant of effective amount, fibrin glue that can delay the releasing of the vasodilating agent. The present invention is characterized in that the composition is a mixture of the fibrin glue and the vasodilating agent; the mixing concentration changes in the range from 0.1mg per ml to 10mg per ml according to various kinds of vasodilating agents. In the present invention, the long acting composition of the fibrin glue vasodilating agent with sustained release property has the following properties of good tissue compatibility, slow releasing of the drugs, long maintenance in the application area and reduction of the side effects to the human body. The present invention is applied in the control during surgery as well as the prevention and treatment after the surgery, which can cause the vasospasm attack. The present invention is particularly applied in the prevention and reduction of the convulsive seizure, which occurs in the coronary artery bypass grafting operation or after the operation. Therefore the pain of the patient is dramatically decreased and the cure rate is improved, and the recurrence is reduced.
CA2194462C Hard tissue stimulating agent The use of chitosan and a polysaccharide immobilized thereto selected from heparin, heparan sulphate, chondroitinsulphates and dextran sulphate for the manufacture of an agent capable of providing stimulated regeneration of hard tissue; a process for stimulating regeneration of hard tissue in connection with so-called osseointegration; and implant intended for integration into hard tissue, particularly bone tissue.
EP2373305A1 Transdermal pharmaceutical compositions comprising a serm The present invention relates to transdermal pharmaceutical compositions such as gels containing a SERM selected from the group consisting of endoxifen, droloxifene, clomifene, raloxifene, tamoxifen, 4-OH tamoxifen, toremifene, danazol and the pharmaceutically acceptable salts thereof, and to methods of making and using the same.
EP1032559B1 Aminoalkylphenol derivatives for treating depression and memory dysfunction Novel aminoalkylphenols, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the aminoalkylphenols or compositions thereof are disclosed.
US20080188447 Glucocorticoid-lowering composition This disclosure relates to a composition comprising pregnane derivatives according to Formula (I), or a salt, solvate or hydrate thereof, and to a pharmaceutically acceptable carrier or excipient. The composition may be used to lower glucocorticoid level in a human or animal. It may also be used tor modulate activity of enzymes of glucocorticoid metabolism, to modulate RNA transcription and protein level of hypothalamic, hippocampal and pituitary peptides, or for treatment or prophylaxis of human or animal diseases.
CN103599547A Nitric oxide donor type non-steroidal anti-inflammatory drug beta-cyclodextrin or beta-cyclodextrin derivative inclusion compound as well as preparation method and application thereof The invention provides a nitric oxide donor type non-steroidal anti-inflammatory drug beta-cyclodextrin or beta-cyclodextrin derivative inclusion compound as well as a preparation method and an application thereof. The nitric oxide donor type non-steroidal anti-inflammatory drug beta-cyclodextrin or beta-cyclodextrin derivative inclusion compound comprises a nitric oxide donor type non-steroidal anti-inflammatory drug and beta-cyclodextrin or a beta-cyclodextrin derivative, wherein the molar ratio of the nitric oxide donor type non-steroidal anti-inflammatory drug to beta-cyclodextrin or the beta-cyclodextrin derivative is 1: 1-1: 25. The inclusion compound has high bioavailability and good stability. The preparation method of the inclusion compound, provided by the invention, has the advantages that that the complete separation of the inclusion compound from medicinal raw materials which are not included is realized, the medicinal raw materials which are not included can be completely recycled, and the cost is reduced. The inclusion rate of the preferable preparation method reaches above 70%.
US20100040700 Kit for promoting hair growth A kit for promoting hair growth on areas of the scalp that has been affected by fungal infections. The kit reduces the loss of hair, gradually destroys the cause of the loss of hair, and eventually restores the normal hair growth in the areas of the scalp affected by the fungi. The kit is comprised of a first powdered mixture and three liquid compositions. The elements of the kit are applied to the scalp of an individual experiencing hair loss due to fungi.
US20110130385 Bicyclic Heterocylic Derivatives and Methods of Use The present invention relates to novel bicyclic heterocycle derivatives, pharmaceutical compositions comprising the bicyclic heterocycle derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is: I, Ia, Ib ou Ic. R2 is alkyl, alkenyl, aryl, cycloalkyl. heterocycloalkyl or heteroaryl, any of which can be optionally substituted with R3; Y is —C(O)—, —S—, —S(O)—, —S(O)2—, —CH2— or —O—, such that if Y is —O— or —S—, then M is other than N and R1 is (Ib);
US20080181880 Inducing rapid bone formation; contains bone anabolic agent and a mechanical alteration device for altering contents of a bone marrow cavity, increase in osteoblast activity; antiresorptive agent for prevent resorption; drug targeting of specific bones A method of inducing bone formation in a subject in need of such inducement comprises the steps of mechanically inducing an increase in osteoblast activity in the subject and elevating blood concentration of at least one bone anabolic agent in the subject. The method steps may be performed in any order, but in sufficient time proximity that the elevated concentration of the anabolic agent and the mechanically induced increase in osteoblast activity overlaps. The method may additionally comprise providing the subject with an elevated blood concentration of at least one antiresorptive agent, wherein the elevated concentration is sufficient to prevent resorption of new bone growth produced due to the osteoblast activity. Use of the method permits targeting of specific bones of the subject for bone production and preservation, faster bone production and earlier discontinuation of bone anabolic pharmaceuticals. Kits adapted for performing the method are provided.
US6838465 N-acyltetrahydroisoquinoline derivatives This invention relates to novel compounds represented by the general formula [I]: (wherein, R1 and R4 are the same or different, and represent hydrogen atoms, lower alkyl groups or the like; R2 and R3 are the same or different, and represent lower alkoxy groups or lower alkyl groups; R5 represents a lower alkyl group or aralkyl group optionally having substituent(s); R6 represents a hydrogen atom or a lower alkyl group; X represents O, S or NH; m represents an integer of 0 to 3; n represents an integer of 0 or 1; and Ar represents a phenyl group or heteroaryl group optionally having substituent(s)). The compounds of the invention have an antagonistic action on orexin receptors, and are useful for treatment of appetite abnormality, obesity, sleeping disorder or the like.
CN103751138A Orally disintegrating tablet containing lasofoxifene tartrate and preparation method thereof The invention belongs to the field of medicinal preparations, and relates to a lasofoxifene tartrate orally disintegrating tablet for treating postmenopausal osteoporosis and a preparation method thereof. Proper medical auxiliaries are selected according to physicochemical properties of lasofoxifene tartrate, and the orally disintegrating tablet comprises a filling agent, a disintegrating agent, a flavoring agent, a lubricant, a glidant and the like. The medicine can be prepared by granulating and tabletting by a wet method, directly tabletting, or granulating and tabletting by a dry method. The invention aims to provide the lasofoxifene tartrate orally disintegrating tablet with simple preparation process, convenience in administration, quick response to indications, exact curative effect and high bioavailability.
US20090017078 Anhydrous topical formulation for polyphenols The present invention discloses a composition of matter, and method to formulate same, which is an anhydrous topical cream, gel or ointment base, a polyphenol and a suitable adsorbent binding carrier to which the polyphenol will bind for purposes of even disbursement within the cream, gel or base and which will not inhibit the ability of the polyphenols to be released on and into the aqueous environment of the skin when the topical mixture is applied thereto. The binding carrier provides the ability to disperse a hydrophilic polyphenol in a non-aqueous medium for purposes of topical application to the body. In particular, the present invention discloses the use of polyphenols such as tea catechins, and in particular green tea catechins, disbursed in an anhydrous base consisting of either saturated or unsaturated plant oils or waxes through the use of a variety of binding carriers including, but is not limited to, talcs and clays, alginates, algae, agars, gums, gelatins, celluloses, silica, silica gels, simethicone, salicylates, silicates and silicone resins, tragacanths, calcium carbonates and magnesium or zinc oxides. Such binding carriers are particularly useful when polyphenol concentrations exceed 0.2% w/w in the mixture, and their use is preferred when concentrations are between 1.0 to 20% w/w polyphenols.
CN1660100A Medication for treating diabetes and complication A medicine for treating diabetes and its complications is prepared from ligustrazine and aminoguanidine.
CN103142826A Poison yam strangury freeing tablet The invention discloses a poison yam strangury freeing tablet, which is characterized in that the poison yam strangury freeing tablet is prepared by using the following raw materials: lilac pink herb, common knotgrass herb, plantain seed, talc, poison yam, rhubarb root and rhizome, amur cork-tree, dandelion, Tokyo violet herb, golden thread, baical skullcap root, Chinese thorowax root and common anemarrhena rhizome.
CN102600176A Application of nilestriol compound in preparing information treatment drug, preparation method and prepared novel drug The invention discloses application of a nilestriol compound in preparing an information treatment drug, a preparation method of the nilestriol compound and a novel drug prepared by the method. During the treatment, the information treatment drug does not directly touch a human body, drug substance components are not consumed, chemotherapy effects can be achieved only by drug information physiotherapy, and the therapy window is enlarged more than one thousand times, and side effects of the chemotherapy are avoided. After nilestriole is used as the information treatment drug, the effective component content is not changed, and nilestriole can be used secondarily and effectively as a chemotherapy normal preparation.
US7053110 Dietetics; osteoporosis; muscular disorders Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably, and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.
US20100197643 Phytochemical-rich oils and methods related thereto The invention relates to methods used in extracting oil from plants, plant fruits, and/or nuts, preferably fruits from plants of the family Arecaceae, or Palmae, even more preferably acai fruit. In some embodiments, the invention relates to methods of extracting the oil using an extraction solution comprising a volatile alcohol and volatile ketone. In other embodiments, the invention relates to oil from acai fruit and acai fruit by-products that contain enriched concentrations of phytochemicals.
WO2010038647A1 Adhesive patch and adhesive patch kit An adhesive patch (1) comprising a backing and a pressure-sensitive adhesive layer (10) formed on one side thereof. The adhesive patch (1) further includes a filmy release liner (2) with which the pressure-sensitive adhesive layer (10) is covered. The release liner (2) can be divided into at least two portions, i.e., a first release liner (21), with which a central part (10b) of the pressure-sensitive adhesive layer (10) is covered, and a second release liner (22), with which two end parts (10a, 10c) of the pressure-sensitive adhesive layer (10) are covered. The second release liner (22) has: a pinching part (22a) with which the pressure-sensitive adhesive layer (10) is not covered; and a pair of supporting parts (22b, 22c) which have been connected to the pinching part (22a) so as to leave a given space (23) therebetween and with which the two end parts (10a, 10c) of the pressure-sensitive adhesive layer (10) are covered. Part of the contour of the first release liner (21) coincides with the contour of the space (23) in the second release liner (22). Other contour of the first release liner (21), together with the contour of the second release liner (22) excluding the space (23), forms the whole contour of the release liner (2).
CN101152179A Application of isoniazide as histone deacetylase inhibitors The invention discloses isoniazid indicated in formula (I), which has a new purpose of being used as histone deacetylase inhibitor. The isoniazid is used to prepare medicine to prevent and/or treat a plurality of diseases related to histone deacetylase.
CN101151032B Pharmaceutical composition and method using antifungal agent in combination A pharmaceutical composition containing one or more antifungal agents selected from an arylamidine derivative represented by the general formula (1), (wherein R<1> represents an amidino group that may be substituted with a hydroxyl group that may be protected with an acyl group, an amidino group that may be substituted with an alkoxy group that may be substituted, or an amidino group that may be substituted with an aralkyloxy group that may be substituted; R<2> and R<3> identically or differently represent a hydrogen atom or a halogen atom) or a salt thereof, an azole antifungal agent, a polyene antifungal agent, a candin antifungal agent and a fluoropyrimidine antifungal agent has a strong antifungal activity and is useful for the treatment of fungal infection. A method for using them in combination is useful as an excellent therapeutic method for fungal infection. A pharmaceutical composition containing the arylamidine derivative represented by the above general formula or a salt thereof and an immunosuppressing agent has a strong antifungal activity and is useful for the treatment of fungal infection and a skin disease such as atopic dermatitis. A method for using them in combination is useful as an excellent therapeutic method for fungal infection and a skin disease such as atopic dermatitis.
CN102813663A Pharmaceutical composition containing tetrahydrofolic acid The present invention relates to solid pharmaceutical compositions, in particular to oral contraceptives, comprising a progestogen, such as drospirenone; an estrogen, such as ethinylestradiol; a tetrahydrofolic acid or a pharmaceutically acceptable salt thereof, such as calcium 5-methyl-(6S)-tetrahydrofolate; and at least one pharmaceutical acceptable excipient or carrier. The compositions of the invention provide good stability of the tetrahydrofolic acid upon storage while still ensuring a fast and reliable release of the estrogen and the progestogen present in the composition.
CN103372201A Hard capsule formula and production method thereof The invention discloses a hard capsule formula and a production method of the hard capsule formula. The hard capsule formula is prepared from the following components by the weight: 80mg of gadus collagen peptide, 60mg of vera aloe extracts, 40mg of soy isoflavone, 50mg of seabuckthorn brass, 50mg of rose extracts, 3mg of food-grade hyaluronic acid, 10mg of vitamins C, 20mg of oligosaccharide, 2mg of compound nutrients and 65mg of auxiliary materials. According to the hard capsule formula and the production method of the hard capsule formula, the hard capsule formula is obtained in the weight proportion, the absorption of medicines is promoted by orally taking capsules so as to physiologically regulating the body to fulfill the aims of whitening, moisturizing and expelling toxin, and the toxic and side effects are avoided. The hard capsule formula has the functions of clearing heat, resisting inflammatory, whitening, moisturizing, resisting oxidization and aging, regulating female inner environment, expelling toxin and beautifying and increasing the skin elasticity.
WO2008112495A1 Synthesis and characterization of polymorph form iii of 4-(2,(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile A polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form III are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. Also provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.
US20080293680 Substituted Ethane-1,2-Diamines for the Treatment of Alzheimer's Disease II The invention relates to a compound of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are defined as in the specification and claims and to its use for treating or preventing Alzheimer's disease and other similar diseases.
CN101537081A Matsutake health-care medicinal liquor with anticancer function and human body immunizing power enhancement function The invention discloses health-care medicinal liquor, in particular to matsutake health-care medicinal liquor with an anticancer function and a human body immunizing power enhancement function and a preparation method thereof, belonging to the technical field of health-care productions. The matsutake health-care medicinal liquor is prepared by the following materials by weight: 500-800 parts of white wine of 40-65 DEG, 2-6 parts of matsutakes, 1-4 parts of medlars, 1-3 parts of panax, 1-4 parts of ganoderma, 1-4 parts of Chinese dates, 0.5-2 parts of longans and 1-5 parts of medical stones. The matsutake health-care medicinal liquor has unique flavor, perfume dispersed all round and mellow mouthfeel, contains crude protein, crude fat, crude fibers, a plurality of vitamins and various amino acids and has optimal anticancer and human body immunizing power enhancement effect by being validated by clinical trials.
CN101953790A Granules comprising cefprozil lipidosome and preparation method thereof The invention relates to cefprozil lipidosome, a preparation method thereof and granules comprising the same. The cefprozil lipidosome comprises the following components in proportion by weight: 1 cefprozi, 1.25-5 hydrogenated soybean lecithin, 1.25-5 egg yolk lecithin, 2.5-10 cholesterin and 0.1-3 vitamin E. The cefprozil granules not only conform to the requirements of Chinese pharmacopoeia, but also has the advantages of more stable storage at normal temperature, faster drug effect-taking, and obviously improved bioavailability compared with the common cefprozil pharmaceutical composition.
US20060199789 medical composition The present invention provides a pharmaceutical composition, which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] or a pharmaceutically acceptable salt thereof and a steroid agent; an agent for treating and/or preventing a pulmonary disease; the agent which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] or a pharmaceutically acceptable salt thereof and a steroid agent which are simultaneously or separately with an interval and the like.
US20050176725 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide; antitumor; antiproliferative agent; synergistic therapy for resistant; Bcr/Abl, leukemia The present invention pertains to a combination for simultaneous, separate or sequential use which comprises (a) a cyclin-dependent kinase inhibitor and (b) 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide and to its use for the treatment of cancer, especially of Bcr/Abl+ leukemia resistant to compound of formula I.
WO2010083725A1 Cephalosporin derivatives containing substituted nitrogen-containing fused heterocyclic ring Compounds of formula I, pharmaceutically acceptable salts, esters, isomers or solvates thereof, wherein R1 and R2 are independently hydrogen, C1-6 alkyl or amino- protecting group; X is N and the like; R3 is H and the like；ring B is a ring with 3 to 8 members; R4 is H,C1-6 alkyl and the like；R5,R6 and R7 are independently hydrogen, C1-6 alkyl and the like or R6,R7 and the atom which they connect form a ring; n is an integer from 1 to 3；and the dotted line represents single bond or double bond. The compounds have good antimicrobial activities and can be effective ingredients of agents for preventing and/or treating infection of respiratory system, otolaryngological department, bone and arthrosis infection caused by bacterial pathogen.
EP1935885A2 Melanin concentrating hormone receptor ligands : substituted 1-benzyl-4-aryl piperazine analogues. Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-arylpiperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
CN101297868A Medicament for preventing and treating osteoporosis and preparation thereof The invention discloses a drug for prevention and treatment for osteoporosis and a preparation method thereof, the product is prepared by pharmaceutical raw materials with the following mix ratio by weight: 0.1 to 10 parts by weight of epimedium herb extract, 0.1 to 10 parts by weight of soybean isoflavone, 20 to 100 parts by weight of ginseng, 20 to 80 parts by weight of Chinese angelica, 10 to 60 parts by weight of lucid ganoderma and 10 to 60 parts by weight of desertliving cistanche; the drug adopts the modern preparation technology and can be processed into any formulation of clinical acceptable tablets, capsules, granules, soft capsules, dispersible tablets and chewable tablets. The drug has the effects of invigorating liver and kidney, strengthening bones and tendons, nourishing essence, filling marrow, replenishing qi and activating blood circulation, which is used for prevention and treatment for the osteoporosis with the symptoms of low back pain, bone pain, flexion of vertebral column, and cramp and so on.
WO2006039704A3 Pharmaceutical composition and method for treating a joint capsule arthropathy A pharmaceutical composition for use in treating a joint-capsule arthropathy comprising an effective amount of one or more of a locally administered, optionally encapsulated therapeutic agent in admixture with a hyaluronic acid delivery vehicle and a method for use thereof in treating a joint-capsule arthropathy by intra-articular injection.
US20090048283 Salt of an androgen receptor modulator The biphthalate salts of compound I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
CN1634121A Dripping pills of ganoderma lucidum polysaccharide and polystictus versicolor polysaccharide The invention relates to a pharmaceutical composition oral preparation which contains polysaccharide of Ganoderma lucidum or krestin as the active component, wherein the medicinal composition can be used for treating various diseases, and has the functions of immunological regulation, anticancer and antisenescence. The medicinal composition also contains a finite proportion of medicinal carrying agent as the substrate.
CN101708249B Buccal tablets used for treating wind-heat acute pharyngitis The invention discloses buccal tablets used for treating wind-heat acute pharyngitis, which is characterized in that the prepared effective components comprise the following raw materials in part by weight: 50 to 200 parts of grosvener siraitia, 30 to 120 parts of honeysuckle flower, 40 to 120 parts of terminalia immature fruit, 20 to 80 parts of figwort root, 20 to 80 parts of indigowoad root, 20 to 80 parts of liquorice root, 0.5 to 3 parts of menthol and 1 to 4 parts of borneol; and the buccal tablets are prepared by adopting a conventional method. The buccal tablets have good mouthfeel, sour and sweet taste and pungent-cold nature, has the functions of dispelling wind and clearing heat, resolving toxin and dispersing swelling, disinhibiting throat and relieving pain, mainly treats thewind-heat acute pharyngitis such as sore throat, scorching hot, hoarseness and dysphagia with a total effective rate of 95 percent, and has no toxin and side effect.
US7763621 3-[[6-[4-(1,2,3,4-tetrahydro-1,8-naphthyridin-7-yl)-1-piperidinyl]-2,5-dimethyl-4-pyrimidinyl]amino]-N-[(phenylmethoxy)carbonyl]alanine, used for the treatment of osteoporosis, restenosis, arteriosclerosis, nephropathy or retinopathy A subject of the invention is the compounds of formula (I): in which R1, R2, R3, R4 and G have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.
CA2279846C Engineered protein kinases which can utilize modified nucleotide triphosphate substrates Engineered protein kinases which can utilize modified nucleotide triphosphate substrates that are not as readily utilized by the wild-type forms of those enzymes, and methods of making and using them. Modified nucleotide triphosphate substrates and methods of making and using them. Methods for using such engineered kinases and such modified substrates to identify which protein substrates the kinases act upon, to measure the extent of such action, and to determine if test compounds can modulate such action. Also engineered forms of multi-substrate enzymes which covalently attach part or all of at least one (donor) substrate to at least one other (recipient) substrate, which engineered forms will accept modified substrates that are not as readily utilized by the wild-type forms of those enzymes. Methods for making and using such engineered enzymes. Modified substrates and methods of making and using them. Methods for using such engineered enzymes and such modified substrates to identify the recipient substrates the enzymes act upon, to measure the extent of such action, and to measure whether test compounds modulate such action.
WO2011023585A1 Piperidine derivatives used as orexin antagonists This invention relates to he teroarylamine methyl substituted piperidine derivatives (I) and their use as antagonists of human orexin.
US20110046080 Composition for Treating a Skin Disorder The present invention relates to the use of a plant of the genus, Capsicum, or part thereof or extract thereof for treating or alleviating the symptoms of a skin condition or disorder, including dermatitis. The present invention also relates to compositions comprising the same for such use, together with methods of treating or alleviating the symptoms of eczema or dermatitis.
US20110223252 Electrolyte purgative The invention relates to compositions for use in purgatives, to purgatives comprising such compositions, and to methods for inducing purgation of the colon. The composition may comprise at least one water-soluble sodium salt; at least one water-soluble minimally degradable sugar in an amount, by weight, of from about 1 to about 3 times the weight of sodium ions in said composition; at least one water-soluble potassium salt in an amount, by weight, of from about 0.05 to about 1 time the weight of said sodium salt in said composition; and at least one water-soluble magnesium salt, wherein the weight of magnesium ions in said composition is from 0.1 to about 10 times the weight of sodium ions in said composition.
US20080139622 Decahydronaphthalene Compounds This invention relates to a compound of the following formula: wherein R1, R2, R3, G, and Z are defined herein. It also relates to is methods of treating autoimmune disease, cancer, and atherosclerosis with such a compound.
WO2006117217A2 Novel use of spiegelmers The invention relates to the use of an L-nucleic acid as an intracellularly active substance.
WO2009050143A1 Combinations of (1r, 2r, 3s, 4s) -n4- (3-aminocarbonylbicyclo [2. 2. 1] hept-5-ene-2-yl) - 5-fluoro-n2- [ ( 3 - methyl-4- (4 -methylpiperazin-1-yl] phenyl-2, 4-pyrimidineamine The invention relates to combinations of (1 R,2R,3S,4S)-N4-(3- aminocarbonylbicyclo[2.2.1]hept-5-ene-2-yl)-5-fluoro-N2-[(3-nnethyl-4-(4- methylpiperazin-1 -yl)]phenyl-2,4-pyrimidinediamine and/or its physiologically acceptable salts and solvates, and other cancer therapeutics, and the use of such combinations for the treatment of cancer.
EP2405909A1 Compositions and methods for elimination of gram-negative bacteria Oral drug delivery formulations which specifically administer antibacterial agents to the ileum, caecum, and/or the colon, without significant administration elsewhere in the gastrointestinal tract, are disclosed. The formulations include, as actives, a combination of a macrolide or aminoglysoside, or quinolone antibacterial and an anti-Gram-negative lipopeptide (polymyxin) antibacterial agent or other peptide antibacterials effective against Gram-negative bacteria. The formulations can be used to treat infections or unwanted colonization in the colon, and to provide effective decontamination of the colonic flora from unwanted or potentially pathogenic bacteria.
CN102791274A Epithelial cell-cell adhesion enhancer, and ameliorating, therapeutic or prophylactic agent for allergic diseases using same Disclosed is a composition containing a specific oligosaccharide and a bivalent metal cation, which exhibits an effect on the amelioration, treatment or prevention of allergy or topical inflammatory reactions in an extremely safe and effective manner compared to synthetic oral steroid medicines in spite of a fact that the composition contains components that are generally familiar as a food or an ion occurring in living bodies and have no toxicity against living bodies when used at physiological concentrations. Specifically disclosed is a cell-cell adhesion enhancer in epithelial cells, which comprises 1-kestose and/or nystose and a bivalent metal cation as active ingredients. The enhancer can prevent the disruption of an epithelial cell-cell tight junction protein that causes the invasion of an allergen into the body, can repair the epithelial cell-cell tight junction protein or promote the formation of the epithelial cell-cell tight junction protein, whereby the epithelial cell-cell adhesion can be enhanced and the effective amelioration, treatment and prevention of allergic symptoms can be achieved.
WO2012123432A1 Sec-hydroxycyclohexyl derivatives as hsl inhibitors for the treatment diabetes The invention provides novel compounds having the general formula (I) wherein R1, R2 and R3 are as described herein, and compositions including the compounds. The use of the compounds as inhibitors of hormone sensitive lipose (HSL) for the treatment of diseases such as diabetes and metabolic symdrome is also disclosed.
CN1847226A Quinolyl amide derivative and its prepn process and use The present invention relates to quinolyl amide derivatives, their preparation process, medicine compositions and use in preparing medicines for treating and/or preventing chronic nephritis, rheumarthritis, insulin dependent diabetes mellitus, systemic lupus erythematous, multiple sclerosis and other diseases.
CN103340876A Application of Asperverin in preparation of drug for treating nasopharynx cancer The invention discloses application of Asperverin in preparation of a drug for treating nasopharynx cancer, which belongs to the technical field of novel drug use. According to in-vitro MTT (Methyl Thiazolyl Tetrazolium) antitumor activity evaluation, the Asperverin is found to have an obvious inhibiting effect for the growth of human nasopharynx cancer cell strains HNE 1, HNE 2, HONE 1 and CNE1, and therefore, the Asperverin can be used for preparing the drug for treating nasopharynx cancer and is good in development application prospect. The use of the Asperverin in preparation of the drug for treating nasopharynx cancer is firstly disclosed; moreover, the inhibitory activity of the Asperverin to the nasopharynx cancer cells is unexpectedly strong.
WO2007033522A1 Capsule formulation containing moxifloxacin and its preparation method A capsule formulation of Moxifloxacin or its salts and/or hydrates, comprises a hydroxpropylmethzlcellulose (HPMC) capsule containing Moxifloxacin, at least one disintegrant and at least one lubricant. Preparation of said formulation comprises : mixing or granulating Moxifloxacin blended with at least one disintegrant and at least one lubricant, then filling the mixture into HPMC capsules. The invented capsule formulation has a stable dissolution rate.
CN100998578A Salbutamol water aerosol used for treating asthma An aquatic aerosol of salbutamol for treating asthma by inhalation is proportionally prepared from salbutamol sulfate, Tween-80, EDTA, VC, acidic substance, sodium chloride, alcohol and water.
WO2013093379A1 Novel pharmaceutical compositions comprising an antibody which binds the human anti-mullerian hormone receptor type ii The invention relates to novel pharmaceutical compositions comprising, as active substance, an antibody which binds the human anti-Mullerian hormone receptor type II (AMHR-II) and an anticancer agent, and also to the therapeutic uses of these compositions.
US20060211025 Molecular signatures of commonly fatal carcinomas This invention provides methods, kits, and algorithms for obtaining molecular signatures of cells based on their gene expression profiles. Devices for carrying out molecular signature analysis of unknown samples are also provided.
US20110142902 Hypoxia Inducing Factor (HIF) Stabilising Glasses The present invention relates to a glass composition formulated to provide the controlled release of certain transition metal ions to regulate the cellular hypoxia pathway and the use of these hypoxia-pathway regulating glasses in medicine and in biomedical research, including in the repair, restoration or regeneration of diseased or damaged tissue.
WO2007045096A1 Oligoheteroaromatic luminiscent assemblies as high-affinity dna sequence-directed ligands The present invention provides a novel class of oligoheteroaromatic assemblies with luminescence characteristics and composition based on integrated polyheterocyclic polyamide oligomers of multiple nitrogen-containing heteroaromatic of the general formula (I) This novel class of compounds of the present invention is capable of binding to targeted DNA sequence in the minor groove, and thus is useful for genomics applications. In particular, the compounds of the invention binds to the DNA at a binding stoichiometry of 2: 1 ternary complexation with very high affinity and sequence selectivity.
CA2688187A1 Method of treament using fused aromatic compounds having anti-diabetic activity Fused aromatic compounds of Formula I are PPAR gamma agonists or partial agonists and are useful for weekly dosing in the treatment or control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
WO2012085645A1 Polymorphs of 3-chloro-4[(2r)-2 Polymorphs of 3-chloro-4[(2R)-2-(4-chlorophenyl)-4-[(1R)-1-(4-cyanophenyl)ethyl]-1- piperazinyl]-benzonitrile are disclosed, as well as pharmaceutical compositions comprising said polymorphs, methods of using the polymorphs, and a process for preparing them.
CN101857564A Method for removing dioxane from Ftibamzone raw material The invention discloses a method for removing dioxane from a Ftibamzone raw material, which carries out recrystallization or solvent reflux on the Ftibamzone raw material to obtain Ftibamzone which does not contain the dioxane. Specifically, the method comprises the steps of: adding the ftibamzone raw material in a latent solvent; heating for dissolving; standing for crystallizing; filtering; and collecting the solvent from obtained crystal and filtrate to obtain residues which are the Ftibamzone which does not contain the dioxane. Or the other technical scheme comprises the steps of : 1. recrystallizing a coarse Ftibamzone product with a mixed solvent of ethanol and dioxane; (2) adding the latent solvent in the obtained crystal for reflux by heating; cooling the reflux liquid and then filtering; and collecting the solvent from an undissolved substance and filtrate to obtain residues which are the Ftibamzone which does not contain the dioxane.
CN102166197A Racecadotril granules and production process thereof The invention relates to the field of medicaments, in particular to racecadotril granules and production process thereof. The racecadotril granules comprise the following components in percentage by mass: 20 to 30 percent of racecadotril bitter masked microcapsule, 70 to 80 percent of filler, 1 to 3 percent of sweetening agent, 0.2 to 1 percent of flavoring agent and 0.8 to 1.5 percent of bonding agent, wherein the racecadotril bitter masked microcapsules comprise the following components in percentage by mass: 3.5 to 5 percent of racecadotril, 3 to 6 percent of sodium alginate, 7 to 10 percent of calcium chloride, 0.8 to 1.5 percent of glycerin and 75 to 88 percent of drying thinner. The invention provides racecadotril granules, which improve the mouthfeel of medicaments, do not affect in vivo dissolution effect of medicaments, use common auxiliary materials as auxiliary materials and do not cause side effects and obvious irritability, and a production process thereof.
WO2011116951A1 Pharmaceutically active disubstituted triazine derivatives The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase. formula (I) wherein R1 is formula (II), formula (III) or formula (IV).
US20060029684 Synergistic treatment of DNA viral infections The synergistic combination of a loop diuretic and lithium is useful in the treatment of DNA viral infections.
US20110124607 Composition for regulation cellular senescence comprising lysophosphatidic acid and inhibitor of adenylyl cyclase as active ingredients The present invention relates to the molecular mechanism inducing cell proliferation in aged human fibroblasts by inhibiting AMPK using LPA and AC inhibitor. Particularly, the present invention relates to a composition comprising LPA and ACI as active ingredients and the invention proves with the said composition that LPA and ACI regulate different phosphorylation of AMPKα and thus inactivate p53 and induce senescent cell proliferation. This results support the fact that AMPK signal transduction plays an important role in cell proliferation of senescent cells.
CN103585106A PH sensitivity modified liposome and its preparation method The invention relates to a pH sensitivity modified liposome, which is prepared by using polyaspartic acid or alicyclic amine graft polyaspartic acid as a liposome modification agent. The pH sensitivity modified liposome has characteristics of uniform particle size distribution, stable performance, remarkable pH sensitivity and good targeting performance. The invention also relates to a preparation method for preparing the above pH sensitivity modified liposome. By electrostatic adsorption between the modification agent and the surface of liposome, liposome can be prepared and simultaneously liposome can be modified by the modification agent. Thus, liposome is prepared by a one-step method, and a lot of preparation time is saved. The method is simple and fast to operate, requires low cost, and has high preparation efficiency.
CA2233975C Succinimide and maleimide cytokine inhibitors Novel succinimides and maleimides are inhibitors or tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is methyl 3-(3',4',5',6'-tetrahydrophthalimido)-(3",4"-dimethoxyphenyl)propionate. The novel compounds have the following formula:(see formula I) in which: R1 is -CH2-, -CH2CO-, or -CO-; R2, R3, R4 and R5 are more fully described in the disclosure.
CN1985987B Medicine composition of glycyrrhizic acid or its salt and reduced glutathione The present invention belongs to the field of medicine technology, and is especially one medicine composition for treating liver diseases and its preparation process and use. The medicine compositionconsists of glycyrrhizic acid or its pharmaceutically acceptable salt 4-800 weight portions, and reductive glutathione 75- 1500 weight portions. The pharmaceutically acceptable salt of glycyrrhizic acid may be metal salt or organic nitrogen salt. The medicine composition may be prepared into different forms. The medicine composition has the synergistic effect of the components in treating liver diseases, high stability, and wide application.
CN102885775A Andrographolide sterile powder and its preparation method The invention relates to the technical field of medicines and discloses an andrographolide sterile powder and its preparation method. The method provided by the invention comprises the following steps of: dissolving an andrographolide raw drug in an alcohol-water mixture or ketone-water mixture at 10-40 DEG C under a D-level aseptic condition, adding active carbon, stirring, carrying out pressure filtration and aseptic filtration under the protection of nitrogen, dropwisely adding an organic solvent into an obtained filtrate at minus 10-20 DEG C for crystallization, and drying to obtain the andrographolide sterile powder. The andrographolide sterile powder prepared by the preparation method has high stability. Addition of auxiliary materials is not required, and safety of clinical use of drugs is increased. The andrographolide sterile powder can be directly packed into a powder injection, which is beneficial to the clinic application of the andrographolide sterile powder.
US8518890 Luteinizing hormone-releasing hormone receptor agonist leuprorelin, or antagonist with androgen receptor agonist for prophylaxis, treatment of prostate cancer; dehydroepiandrosterone, testosterone, dihydrotestosterone; non-steroidal androgen receptor agonist; estradiol, estrone, estriol, stilbestrol A combination agent containing an LHRH receptor agonist or antagonist and an androgen receptor agonist, which is useful as an agent for the prophylaxis or treatment of hormone-dependent diseases and the like, is provided.
WO2007048066A3 Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators A compound according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R6, R7 and Z are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
CN103261203A 6-amido derivatives of 4,5a-poxymorphinans for treatment of pain Compounds of formula: in which R4 is chosen from substituted phenyl, optionally substituted naphthylene, optionally substituted anthracene and optionally substituted aromatic heterocycle, are useful as analgesics.
EP2419084A2 A medicinal cream made using clotrimazole and chitosan and a process to make the same The present invention is directed to a composition for treating fungal skin infections, along with skin rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, and an antifungal active ingredient. It discloses a composition for treating fungal skin infections along with skin rejuvenation containing a) a biopolymer in the form of chitosan, b) an active pharmaceutical ingredient (API) composition in the form of clotrimazole used in treating fungal skin infections, c) a cream base containing primary and secondary emulsifiers, waxy materials, co -solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants and d) water. The active ingredients, namely chitosan, and an anti fungal agent in the form of clotrimazole, are incorporated in cream base for use in treating fungal skin infections with allergy & itching, & wounds on human skin involving contacting human skin with the above identified composition.
US20080167216 for treating Parkinson's disease in a mammal, comprising:providing a quantity of a viral vector expressing an N-terminal of sonic hedgehog ("ShhN"); andadministering a therapeutically effective amount of the quantity of viral vector to the mammal. Described herein are compositions and methods for the treatment of Parkinson's disease (PD) and/or to protect dopaminergic nigrostriatal neuronal cell bodies from 6-OHDA-induced neurotoxicity in a mammal. In various embodiments of the invention, the dopaminergic neuron differentiation factor sonic hedgehog (Shh) and/or its downstream transcription factor target Gli-1 are used in connection with gene therapeutic techniques or direct peptide injection for the aforementioned indications. Kits useful in practicing the inventive method are also disclosed, as are animal models useful for studying various neurodegenerative conditions.
WO2010040272A1 Amide compounds, their pharmaceutical compositions, their preparation and their use The present invention belongs to pharmaceutical chemistry field and discloses 8-(3-aminopropyl)-3-exo-8-azabicyclo[3.2.1]octane-3-amino amide compounds shown as the following formula I, their pharmaceutical compositions, their preparation and their use. Such compounds or their pharmaceutically acceptable salts can be used as CCR5 inhibitors and can be used in preparing the medicaments for treating diseases mediated by CCR5, especially in preparing the medicaments for treating HIV infection, asthma, rheumatoid arthritis, autoimmune disease and chronic obstructive pulmonary disease (COPD).
CN1813716A Use of indole-2,3-dione for preparing medicine for cardio-cerehral vascular disease The present invention discloses an application of indole-2.3-diketone (MW147) in preparation of medicine for preventing and/or curing angiocardiopathy and cerebrovascular disease. Said MW147 has the action of preventing formation of AS and promoting repercussion of AS, so that it can be made into the medicine for resisting As.
CN101939030A Use of alginate oligomers in combating biofilms The invention provides a method for combating biofilm, said method comprising contacting a biofilm with an alginate oligomer. The biofilm may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use in the treatment or prevention of a biofilm infection in a subject. In another aspect the method can be used to combat biofilms, on abiotic surfaces, e.g. for disinfection and cleaning purposes.
WO2006079474A1 Prevention and treatment of thromboembolic disorders The present invention relates to the field of blood coagulation, more specifically it relates to a method of treating a thromboembolic disorder by administering once daily a direct factor Xa inhibitor in oral dosage form to a patient in need thereof, wherein the factor Xa inhibitor has a plasma concentration half life indicative of a bid or tid administration interval, e.g. of 10 hours or less.
EP2269576A2 A Treatment solution and method for preventing posterior capsular opacification by selectively inducing detachment and/or death of lens epithelial cells A treatment solution used to prevent posterior capsular opacification is applied or introduced into the lens capsular bag before, during, or after cataract surgery. The treatment solution may also be applied to the intraocular lens prior to surgery. The treatment solution comprises an ion transport mechanism interference agent, which either alone or in combination with other treatment agents such as an osmotic stress agent to establish a suitable pH, selectively induces detachment and/or death of lens epithelial cells such that posterior capsular opacification is prevented. While the ion transport mechanism interference agent is capable of interfering with the cellular mechanisms and cell ion distribution of a broad range of cells, a concentration of agent is selected such that the treatment solution interferes selectively with the cellular mechanisms of lens epithelial cells while leaving other ocular cells substantially unharmed. The treatment solution selectively induces cellular death and/or detachment of lens epithelial cells while other ocular cells and tissue substantially unharmed and without lengthy preoperative pretreatment.
US20090076130 Compounds for the inhibition of histone deacetylase The invention relates to a compound represented by the following formula (I): and pharmaceutically acceptable salts, stereoisomers, enantiomers, prodrugs and solvates thereof. The compounds are useful as an agent for enhancing the neurite outgrowth and preventing or treating of diseases associated with HDAC in particular, tumor or cell proliferative diseases. In particular, the compounds of the invention can be used as an agent for anti-neurodegenerative diseases and human spinal muscular atrophy (SMA).
CN103463070A Application of Lycojaponicumin C in preparation of medicines for treating breast cancer The invention discloses an application of Lycojaponicumin C in the preparation of medicines for treating breast cancer, belonging to the technical field of new applications of medicines. The evaluation on an in vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anti-tumor activity shows that the Lycojaponicumin C also has an obvious inhibiting effect on the growth of human breast cancer cell lines 4T1, MCF-7, MDA-MB-231 and MCF-7B. Therefore, the Lycojaponicumin C can be used for the preparation of the medicines for resisting the breast cancer and has good development and application prospects. The application of the Lycojaponicumin C in the preparation of the medicines for treating the human breast cancer is disclosed for the first time. As the skeleton type of the Lycojaponicumin C belongs to a brand-new skeleton type, the Lycojaponicumin C has unexpected strong inhibitory activity on breast cancer cells.
CA2214070C Dihydronaphthalene and naphthalene compounds, intermediates, formulations, and methods The instant invention provides dihydronaphthalene and naphthalene compounds, intermediates, formulations, and methods for use in the treatment of bone loss or bone resorption
WO2013052889A1 Nasal delivery mechanism for prophylactic and post-acute use for progesterone and/or its enantiomer for use in treatment of mild traumatic brain injuries Compositions and methods for treating traumatic brain injury (TBI) and mild traumatic brain injury (mTBI) using progesterone and ent-progesterone are described.
CN102178925A Novel eyesight protective agent lutein ophthalmic preparation The invention discloses a lutein ophthalmic preparation for protecting eyesight, which is prepared from the following raw materials: 5 to 13 parts of water-soluble lutein (based on C4oH56O2), 50 to 80 parts of taurine, 0.1 to 0.5 parts of selenium (based on Se), 10 to 25 parts of zinc (based on Zn), 0.5 to 1.0 part of water-soluble vitamin A, and 0.8 to 2.0 parts of glutathione; an auxiliary material consists of a diluent, a wetting agent, an isoosmotic adjusting agent, a preservative, an antioxygen and water for injection; formulations comprise eye drops, eye lotion and the like; and the lutein ophthalmic preparation is suitable for eye diseases such as myopia, long sight, cataract, glaucoma, retinal pigment degeneration, macular degeneration and the like. Various nutritious factors are reasonably compatible, a blank of a lutein external preparation is filled, and the bioavailability and health-care effect are obviously improved; and through actual application by 300,000 people, the total effective rate for the myopia, cataract and diabetic eye disease is over 90 percent and the lutein ophthalmic preparation has positive promotion valve.
CN1872828B Monocyclic polysubstitution cyclohexenol, and compound of ketones, and preparation method, and usage This invention relates to a polysubstituted monocyclohexenol and ketone compound, extract containing the compound, and its preparation and application. The compound can be used as the cell cycle inhibitor, cell apoptosis inducer, cell proliferation inhibitor and antitumor drug.
WO2010072147A1 Benzisoxazole piperidinyl derivatives, pharmaceutical compositions comprising the derivatives and their use The invention provides benzisoxazole piperidinyl derivatives, their salts and their hydrates: Wherein R, X, Y, R’ and T have the same definition as that described in the description. The kind of compounds has antagonistic effect on 5-HT2A and has mediating effect on 5-hydroxytryptamine system such as reuptake inhibiting effect of 5-HT and so on. The compounds of the present invention possess excellent analgesia, sedation activity, minimal toxicity and side effects. The invention also provides pharmaceutical compositions comprising the derivatives and their use.
WO2007098384A2 Tetracyclic steroid derivatives useful as progesterone receptor modulators The present invention is directed to tetracyclic steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.
US20110160197 Substituted Indoles and a Method for the Production and Use Thereof The invention relates to novel substituted indoles, to the use thereof in the form of pharmacological composition substances and to use of said composition for producing medicinal preparations used for preventing and treating viral diseases, in particular caused by viruses of infectious hepatitis (HCV, HBV), human immune deficiency (HIV), atypical pneumonia (SARS) and bird flu. The invention proposes novel substituted indoles of general formula (1) or the racemates or the optical isomers or the pharmaceutically acceptable salts and/or hydrates thereof, wherein R1, R1 4 and R2 4 independently of each other are an aminogroup substituent selected for hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl, or R1 4 and R2 4 together with a nitrogen atom, with which they are bound, form through R1 4 and R2 4 optionally substituted azaheterocyclyl or guanidyl; R2 is analkyl substituent selected from hydrogen, an optionally substituted mercaptogroup, optionally substituted aminogroup and optionally substituted hydroxyl; R3 is lower alkyl, R5 is an hydrogen atom or R5 together with an oxygen atom with which it is linked or R2 4 together with a nitrogen atom with which it is linked close, via R5 and R2 4 an oxazine cycle; R6 is a cyclic system substituent selected for hydrogen, a halogen atom, cyanogroup, optionally substituted aryl or substituted heterocyclyl.
CN103127056A Application of psoromic acid in anti-tumor drug preparation The invention belongs to the field of chemical engineering and medicine, and relates to an application of psoromic acid in anti-tumor drug preparation. The present invention provides an application of psoromic acid in anti-tumor drug preparation, wherein tumor cells comprise liver cancer cells, leukemia cells and pancreatic cancer cells. The psoromic acid belongs to natural products, and has characteristics of low toxic-side effect, high bioavailability, stable property, and clinical use value. With application of the small molecule compound as a new anti-tumor drug or an auxiliary component thereof to be developed, advantages of significant tumor inhibition effect and green environmental protection are provided, and a new way is provided for treatment and cure of tumors.
US20110280928 Wound Care Device Having Fluid Transfer Properties This disclosure relates to wound care devices which are capable of one-way, directional flow of fluids and contaminants away from the wound site to the opposite side of the wound care device, which functions as a fluid reservoir. This fluid transport mechanism generally aids in reducing wound maceration by removing excess fluid, and potentially even bacteria, and is carried out without loss of physical integrity of the wound care device itself. In addition to providing a uni-directional fluid transport mechanism, the wound care device may contain a topically applied silver-based antimicrobial finish which provides certain levels of antimicrobial agent to the wound in order to clear infection from the wound site and control bacterial growth in the wound care dressing. Exemplary topical antimicrobial finishes include silver ion-releasing compounds.
WO2007042272A2 Use of a nutraceutical composition comprising resveratrol for the treatment of age-related diseases The use of resveratrol, a derivative, metabolite or analogue thereof, in combination with at least one additional component selected from EGCG, coenzyme Q-IO, genistein, lycopene, hydroxytyrosol and polyunsaturated fatty acids in the manufacture of a nutraceutical composition for delaying aging and/or for the treatment or prevention of age-related diseases in animals, in particular in mammals including humans.
WO2014032735A1 Use of 3-(2,2,2-trimethylhydrazinium)-ethylpropionate or a pharmaceutically acceptable salt for treating high tension glaucoma The invention provides the use of 3-(2,2,2-trimethylhydrazinium)-ethylpropionate or a pharmaceutically acceptable salt in the treatment of increased intraocular pressure.
EP2260860A1 Calcium phosphate delivery vehicles for osteoinduktive proteins A composition for treating a mammal having a bone defect. The composition comprises an osteogenic protein, a calcium phosphate material as a carrier, and an effective amount of an effervescent agent. Methods of making the compositions and methods of using the osteogenic compositions to treat osteoporotic and/or osteopenic bone are also disclosed.
WO2012129227A1 Dendritic cells (dcs) targeting for tuberculosis (tb) vaccine Compositions and methods comprising high affinity monoclonal antibody conjugates against several DC receptors are described herein. The inventors prepared fusion proteins with antigens for DC-targeting vaccine generation by conjugating several M. tuberculosis protein antigens with high affinity monoclonal antibodies against several DC receptors with a view to developing novel human vaccines based on in vivo DC-targeting. The findings of studies described herein indicate that vaccines bearing TB antigens can recall a potent memory antigen-specific T cell response in vitro resulting in IFNy secretion.
CN101366719A Triterpenes anti-AIDS drugs The invention discloses a natural medicine having the function of resisting AIDS virus HIV-1. The medicine is a triterpene compound and can be prepared into a medicinal preparation for treating HIV-1 infected persons and AIDS patients.
US7196088 5-HT6 modulators; such as 2-benzenesulfonyl-5-piperazin-1-yl-1,2,3,4-tetrahydroisoquinoline; The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein, n, X, Y, R1, R2, R3, R4 and R5 are as defined herein. The subject compounds are useful for treatment of 5-HT6 receptor antagonist-mediated diseases. Also provides are methods for preparing, compositions comprising, and methods for using the subject compounds.
US7956036 Polypeptide and DNA thereof useful as a neovascular marker A marker for neovascularization, vascular disease, inflammatory disease, entoptic neovascular disease, reproductive system disease, central nervous system disease and cancer, the method of detection of the marker and a diagnosis kit of the diseases are provided. Additionally, therapeutic agents of the diseases are provided. The expression of KIAA1036 is enhanced in ovarian cancer and large bowel cancer and KIAA1036 expresses in umbilical vein endothelial cell and inhibits DNA synthesis in the cells, cell migrating and lumen formation. Therefore KIAA1036 is useful as a marker for neovascularization, vascular disease, inflammatory disease, entoptic neovascular disease, reproductive system disease, central nervous system disease or cancer. Additionally, KIAA1036 is useful for screening of agonists, antagonists, DNA synthesis inhibitors, cell migrating inhibitors and neovascular inhibitors. The substances obtained by the screening, KIAA1036 and the antibodies are useful as therapeutic agents the above disease.
US20070258988 Identification and Characterization of Multiple Splice Variants of the Mu Opioid Receptor Gene The present invention encompasses novel splice variant forms of the mu-opioid receptor-1 (MOR-1) and the polynucleotide sequences encoding the MOR-1 splice variants. The invention further encompasses methods of screening for compositions regulating the MOR-1 splice variant activities and the development of therapeutic modalities directed to regulating activity. Regulation of the MOR-1 splice variant activities may impact the physiologic process of analgesia.
WO2009108272A1 5-hydroxy-2-methyl-4h-pyran-4-one-esters as novel tyrosinase inhibitors Skin brightening compositions based on esters of 5-hydroxy-2-methyl-4H- pyran-4-one. Also disclosed are methods of making the compositions as well as methods of using the compositions.
WO2014089904A1 Triazinone compounds The invention provides a compound of Formula (I), pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
US20090226375 MICRO-RNAs THAT MODULATE SMOOTH MUSCLE PROLIFERATION AND DIFFERENTIATION AND USES THEREOF The present invention relates to the identification of microRNAs that regulate smooth muscle cell proliferation and differentiation, including the miR-143/miR-145 cluster. Methods of treating restenosis and neointima formation by increasing expression of miR-143 and/or miR-145 are disclosed. The present invention also relates to the identification of two microRNAs, miR-486 and miR-422a, that regulate cell survival in the heart. Methods of treating or preventing cardiac hypertrophy, heart failure, or myocardial infarction by increasing expression of miR-486 and/or miR-422a in heart tissue are also disclosed.
CN102198108A Process for preparing Cinacalcet hydrochloride tablets or capsules The invention discloses a process for preparing Cinacalcet hydrochloride tablets or capsules and belongs to the technical field of medicinal preparations. The preparation process comprises performing dry-process granulation according to one formula; and tabletting or filling capsules by using three dosages according to a ratio. The in-vitro release of the Cinacalcet hydrochloride is characterized in that: 40 to 80 percent of Cinacalcet hydrochloride is released within 5 to 10 minutes; 80 to 90 percent of the Cinacalcet hydrochloride is released within 15 to 20 minutes; and 90 to 100 percent of Cinacalcet hydrochloride is released within 30 to 45 minutes. In the process, the procedures are simple and safety, the quality is controllable, the cost is low, and the production period is short. The process is suitable for large-scale industrial production.
CN101401797A Effervescent tablet containing imatinib mesylate and preparation method thereof The invention relates to the technical field of pharmaceutical preparation, in particular to an effervescent tablet containing imatinib mesylate and a method for preparing the same. The effervescent tablet comprises 25 to 500 milligrams of the imatinib mesylate and an acid base pair which is acceptable in pharmacy; furthermore, a filling agent, an adhesive, a disintegrating agent, a lubricating agent, a sweetening agent and a flavour modifying agent which are acceptable in pharmacy can be added in the effervescent tablet. The effervescent tablet containing the imatinib mesylate has the advantages of faster action speed compared with the tablets and capsulated drugs in the market, has convenient use and good taste in taking, and is more suitable for children, the elderly, and patients who can not swallow solid medicines.
US20110281941 Combination of lycopene, polyphenol, and vitamins for the care of keratin materials The present invention relates to the cosmetic use, by the oral route, of a combination of lycopene, of vitamin C, of vitamin E and of at least one polyphenol compound derived from pine bark as active ingredient intended for maintaining and/or restoring the biomechanical properties of keratinous materials, and notably of the skin.
US20090318489 Aporphine compounds and pharmaceutical use thereof The present invention discloses novel aporphine derivatives. Also, the present invention discloses that these novel aporphine derivatives can be used for treating oxidative stress induced diseases such as cardiovascular disease, diabetes, aging, Alzheimer's disease, kidney disease, cancer or brain ischemic disease etc.
WO2008020617A1 Process for production of brominated acetophenone Disclosed is a process for producing substantially pure 2-bromo-1-arylethanone. The process is characterized by conducting a reaction shown by the scheme below in an alcohol. [Chemical Formula 1] (I) STEP 1 (II) wherein R1 represents a C1-C3 alkoxy group.
US7183272 Crystal forms of oxcarbazepine and processes for their preparation The present invention provides for new crystal forms of oxcarbazepine, more particularly oxcarbazepine Forms B, C, D and E. The present invention further provides processes for preparation of these forms. Form B is prepared by evaporating the solvents from a solution of oxcarbazepine in toluene and dichloromethane. Form B is also obtained by immediately cooling the solution of oxcarbazepine and toluene. Cooling the same solution at a slower rate, but still fairly rapidly, results in oxcarbazepine Form C. Cooling the same solution at even a slower rate results in another Form, oxcarbazepine Form D. Oxcarbazepine Form E, a solvate of chloroform, is obtained by precipitating a solution of oxcarbazepine and chloroform. The present invention also provides processes for converting one of the newly discovered crystal forms of oxcarbazepine into another crystal form, including Form A, which is in the prior art. These conversions may occur by storage at ambient temperature, by heating one particular Form or treatment with a protic solvent.
US20120071430 Synthetic analogs of bacterial quorum sensors Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.
CA2554420A1 Topical otic compositions and methods of topical treatment or prevention of otic infections A topical otic composition containing an azalide antibiotic. A topical otic composition containing an azalide antibiotic and a medicament. A topical otic composition containing an azalide antibiotic and a polymer suspending agent. And methods for treating of preventing infections in the ear using azalide antibiotic compositions.
CN1857388A Preparation and application of notoginseng stem and leaf total saponin composition The present invention relates to compound preparation with total notoginseng stem and leaf saponin composition as main component for treating cardiac and cerebral vascular diseases. The total notoginseng stem and leaf saponin composition contains total notoginseng stem and leaf saponin in 1-99 wt% and pueraria flavonid, total erigeron braviscapus flavone, total astragalus saponin or total salvianolic acid in 1-99 wt%, and is compounded with pharmaceutically acceptable supplementary material to prepare pharmaceutically acceptable preparations. The medicine of the present invention is used in preventing and treating cardiac and cerebral vascular diseases, senile dementia, and other diseases.
WO2006073360A1 NEW USE OF 11-PIPERAZIN-1-YLDIBENZO [b,f] [1,4] THIAZEPINE OR ITS PHARMACEUTICALLY ACCEPTABLE SALT AND TO ORAL PHARMACEUTICAL COMPOSITIONS A method of treating at least one symptom or condition associated with but not limited to: 1) Substance-Related Disorders including but not limited to Substance Dependence, Substance Abuse, Substance Intoxication, Substance Withdrawal, Alcohol-Related Disorders, Amphetamine (or Amphetamine-Like)-Related Disorders, Caffeine-Related Disorders, Cannabis-Related Disorders, Cocaine-Related Disorders, Hallucinogen-Related Disorders, Inhalant-Related Disorders, Nicotine-Related Disorders, Opioid-Related Disorders, Phencyclidine (or Phencyclidine-Like)-Related Disorders, and Sedative-, Hypnotic- or Anxiolytic-Related Disorders. 2) Attention-Deficit and Disruptive Behavior Disorders. 3) Eating Disorders. 4) Personality Disorders including but not limited to Obsessive-Compulsive Personality Disorder. 5) Impulse-Control Disorders, comprising administering an effective amount of Formula I (I) or its pharmaceutically acceptable salt. In another aspect of the invention a pharmaceutical composition is provided comprising an effective amount of Formula I or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable carrier or diluent.
US20120183521 Equine nutritional supplement A nutriceutical supplement for use in equines provides enhanced mitochondrial energizing activity and reduced inflammation and results in enhanced resistance to training injuries and diseases and enhances peak racing performance. The supplement is provided along with equine feed as a formulation including at least Coenzyme Q10, Carnitine, d-Ribose, Boswellia extract and Curcumin. These ingredients provide enhanced mitochondrial energizing activity and reduced stress, inflammation and injuries.
CN1757391A Application of neutral berberine sulfate for preparing medicine to treat and prepvent endotoxic diseases An application of the neutral berberine hydrochloride in preparing the medicines for preventing and treating the endotoxin-type diseases and helping the treatment to heart failure, serious wound, burn and hepatism.
US7150867 Radionuclide-coated particulate material This invention relates to a particulate material comprising an inorganic low density, radiation tolerant core coated with a radionuclide, processes for its production and a method of radiation therapy utilizing the particulate material.
CN102670637A Cholagogue drug for treating hepatitis The invention discloses a cholagogue drug for treating hepatitis, which is made of raw materials which are 25% to 75% by weight of active ingredients gentiopicroside and 25% to 75% by weight of baicalin according to a conventional preparation method. The cholagogue drug for treating the hepatitis can obviously restrain auricles of mice and digits of rats to swell, and reduces times of twisting body and time of swinging tail of the mice, thereby obviously increasing bile secretory volume of the mice and the rats, being capable of effectively prolonging anoxia survival time of the mice, having obvious anti-inflammatory analgesic action of the mice and the rats, and having obvious differences in statistical treatment results (P<0.01-0.05). A composition of the gentiopicroside and the baicalin is made into various common preparation types such as tablets, capsules, powder, pills, granules, injection and emulsion and the like.
EP2391717A1 Treatment of radiation-induced fibrosis The present invention relates to treatment or prevention of radiation induced fibrosis using TNF-alpha antagonism. Preferably, TNF-alpha is antagonized by direct binding or by inhibition of synthesis. In a preferred embodiment, the invention comprises intraperitoneal administration of a chitosan-siRNA nanoparticle, wherein the siRNA is targeted to the mRNA encoding TNF-alpha.
US7641924 Proteins, lipids and carbohydrates including glucose and fructose heterodisaccharides; slow hydrolysis A nutritional composition for controlling blood sugar level comprising a protein, a lipid and a carbohydrate, wherein energy percentages supplied by the protein, lipid and carbohydrate are 10 to 25%, 20 to 35% and 40 to 60%, respectively; and oleic acid in the lipid energy percentage is 60 to 90% and palatinose and/or trehalulose in the carbohydrate energy percentage is 60 to 100%. The composition is useful as an oral or tube feeding nutrient for nutritional management or blood sugar level control of patients suffering from diabetes and glucose intolerance, or for obesity prevention, a therapeutic diet, a diet for diabetic patients at home, an obesity preventive diet or a food with health claims.
CN102311452A Cefixime crystal, preparation method thereof and tablet composition containing same The invention relates to a cefixime crystal, a preparation method thereof and a tablet composition containing the crystal. The cefixime crystal can significantly improve the stability and dissolvability. The tablet core of the cefixime tablet composition is prepared by the following components: 35-65 parts of cefixime crystals, 17-29 parts of starch, 3-6 parts of hydroxypropyl cellulose, 3-5 parts of carboxymethyl starch sodium, 7-13.5 parts of microcrystalline cellulose, 0.3-0.7 parts of starch sodium, and 0.3-0.7 parts of magnesium stearate. The cefixime tablet combination prepared by the invention has good stability, and stable effective component contents, and is an ideal cefixime preparation.
CN102451323A Flesh-engendering powder The invention relates to the technical field of medicine, and provides flesh-engendering powder. The flesh-engendering powder is an externally applied drug which can fast promote wound healing. The flesh-engendering powder is prepared by mixing 40 to 50 parts by weight of calcined gypsum, 5 to 10 parts by weight of calcined dragon's bone, 1 to 5 parts by weight of safflower, 1 to 5 parts by weight of dragon's blood, 5 to 10 parts by weight of nacre, 1 to 5 parts by weight of red halloysite, 5 to 10 parts by weight of amber, 1 to 5 parts by weight of cinnabar, 5 to 10 parts by weight of red sage root, 10 to 15 parts by weight of Chinese angelica, 5 to 10 parts by weight of garden burnet, 1 to 5 parts by weight of elephant hide, and 1 to 5 parts by weight of borneol. The flesh-engendering powder has the advantages of advanced and unique formula, simple processes, simple use method, short onset time, and high cure rate.
WO2013139724A1 Combination therapy (vemrufenib and a mdm2 inhibitor) for the treatment proliferative disorders The present application discloses a product comprising (i) as a first component vemurafenib, and (ii) as a second component an MDM2 inhibitor selected from compounds (II) or (III), or a pharmaceutically acceptable salt thereof, for the sequential or concomitant use in the treatment of proliferative diseases, such as cancer, involving b-Raf V600 mutant positive tumor.
EP2065369A1 Urea compound or salt thereof [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.
WO2011146287A1 Pyrazolo[4,3-b]pyridine-7-amine inhibitors of alk5 The present invention provides ALK5 inhibitors of the formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, methods of making the compounds and intermediates thereof; and methods of using the compounds.
WO2013159006A1 Polymorphs of (s)-1-(4,4,6,6,6-pentadeutero-5-hydroxyhexyl)-3,7-dimethyl-1h-purine-2,6(3h,7h)-dione The present invention provides in one embodiment individual crystalline polymorphs of (S)-1-(4,4,6,6,6-pentadeutero-5-hydroxyhexyl)-3,7-dimethyl-1H-purine- 2,6(3H,7H)-dione designated Form 1, Form 2, Form 3 and Form 4. Each polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data ("XRPD"); (b) differential scanning calorimetry ("DSC"); and (e) thermogravimetric analysis (TGA).
CN101503439A Nucleic acid molecule SI-CYPJ-52 and use thereof in anti-cancer medicine preparation The invention belongs to the biological medicine field, relating to nucleotide molecules and the application thereof in the preparation of antitumor medicines. The invention provides the nucleotide molecules for preparing the antitumor medicines. The nucleotide molecules have the activity for inhibiting the tumor growth and the sequence thereof comprises 5'-CCAGCAAUUUGUCAAGUUA-3' or 5'-CCAGCAATTTGTCAAGTTA-3' which is known as SI-CYPJ-52 in the invention. The nucleotide molecules SI-CYPJ-52 can obviously inhibit the tumor cell proliferation; when the nucleotide molecules are applied to a naked mouse, the tumor body growth of the naked mouse is obviously inhibited compared with the control naked mouse in the same condition of culture, and the phenomenon becomes obvious day by day as time goes on. The invention provides a new approach and means for the tumor treatment and mitigation.
WO2008150191A1 Anorexigenic medicinal agent for controlling the body mass The invention relates to medicine, in particular to pharmacy. The invention consists in using 2,3,3a,4,5,6,-hexahydro-8-cyclohexyl-1H-pyrazino(3,2,1-j,k) carbazole (tetrindole) or pharmaceutically acceptable salts thereof for producing an anorexigenic medicinal agent for controlling the body mass. Tetrindole was known before as a preparation for treating depressions of different genesis. The tetrindole when used for course treatment, exhibits properties making it possible to control the body mass in terms of the reduction thereof. Said preparation is effective and does not exhibit pronounced side effects. An anorexigenic pharmaceutical composition for controlling the body mass containing the effective quantity of the above-mentioned active component and a pharmaceutically acceptable carrier is also disclosed.
CN1582934A Nano micro granules, their preparation and medicinal uses of campotothecin derivative A nanoparticle of camptothecin derivative for preparing the antineoplastic medicines is prepared from gycol-poly-gamme-benzylglutamic acide block copolymer and camptothecin, and is composed of the hydrophobic core and the hydrophilic shell.
US20120070505 Functional amphipilic molecule or macromolecule formulations with multiple compartments The invention relates to novel functional amphiphilic molecule or macromolecule formulations with multiple compartments for transporting or targeting at least one therapeutic agent, in particular an antitumor agent, as well as to a method for preparing such formulations and to the use thereof.
US7135162 Agent for diagnosing and treating malignant tumors A composition of a compound or derivative thereof in which at least one carbon atom of 5-aminolevulinic acid is a carbon isotope and/or a nitrogen atom in its amino group is a nitrogen isotope, and where said derivative is an ester, amide, salt, hydrate or solvate of the compound, and a diagnostically acceptable carrier. A method for detecting malignant tumors, by administering a tumor detecting effective amount to a host in need of tumor detection of a compound or derivative thereof in which at least one carbon atom of 5-aminolevulinic acid is a carbon isotope and/or a nitrogen atom in its amino group is a nitrogen isotope, and where said derivative is an ester, amide, salt, hydrate or solvate of said compound and detecting the malignant tumors using NMR.
WO2013148103A1 Novel compounds for preventing and/or treating lysosomal storage disorders and/or degenerative disorders of the central nervous system Described are novel salts of the compound (3R,4R,5S)-5-(difluoromethyl) piperidine-3,4-diol, as well as methods of using the same for preventing and/or treating lysosomal storage disorders and/or degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease and/or Parkinson's disease.
US20070207148 Genes associated with obesity and methods for using the same The instant invention is concerned with genes associated with obesity. Additionally, the invention provides methods of using the differential expression of these genes associated with obesity to diagnose and treat obesity, as well as to screen for compounds useful for treating obesity.
WO2007016390A1 Matrix metalloproteinase inhibitors for treating fatty liver disease The present invention relates to a method for treating a fatty liver disease or disorder in a patient in need thereof. The method comprises administering at least one matrix metalloproteinase ('MMP') inhibitor to the patient. Fatty liver disease or disorders include, for example, NAFLD, NASH, ALD, fatty liver associated with chronic hepatitis infection, TPN, steroid treatment, tamoxifen treatment, gastrointestional operations, diabetes and Reye's Syndrome. The method is particularly useful when the fatty liver disease is associated with TPN and the patient is an infant or when the patient is obese. MMP inhibitors useful in the present invention include, for example, Marimastat, tetracyclines, Prinomastat, Batimastat, BAY 12-9566, AG3340 , BMS-275291, Neovastat , BB-3644, KB-R7785, TIMPl, TIMP2, doxycycline, minocycline, RS-130,830; CGS 27023A, Solimastat, Ro 32-3555, BMS-272591, and D2163. Marimastat is a preferred MMP inhibitor.
CN101062418A Cyclodextrin inclusion compound of entecavir, the preparing method and the medicine combination including the same The invention discloses a cyclodextrin inclusion compound of Entikawe, which is characterized by the following: incorporating the Entikawe in water-soluble cyclodextrin with mole ratio at 1 : 1-1 : 100; also providing a preparing method and medicinal compound with this inclusion compound. This product simplifies the preparing craft, which is fit for industrial production.
CN101732579B Medicinal composition for treating rheumatism and rheumatoid arthritis The invention discloses a medicinal composition for treating rheumatism and rheumatoid arthritis. The medicinal composition consists of more than 20 medicaments, such as fortune's drynaria rhizome, processed nux vomica, scorpion, himalayan teasel root, frankincense, myrrh, diversifolious patrinia root and the like and has no side effect of chemical medicaments. The medicinal composition has the effects of drilling tendon, penetrating bone, activating tendons, expelling wind, relieving pain and eliminating stagnation and has the remarkable treatment effects of treating the rheumatism, the rheumatoid arthritis, scapulohumeral periarthritis, sciatica, gout, cervical spondylosis, herniated disk, hyperosteogeny, osteonecrosis and lupus erythematosus.
US20130045953 Nestorone®/estradiol transdermal gel The invention discloses compositions and methods for ensuring in both women of fertile age where it ensures also a contraception with additional health benefits and in postmenopausal women where it offers a hormonal therapy with additional medical benefits such as the potential for lower risk of thrombosis. The aforementioned compositions comprising NES as a potent progestational and antiovulatory agent with no androgenic nor estrogenic nor glucocorticoid effect, and combined with estradiol formulated for non-oral transdermal administration as specific daily doses.
US20070275067 Compression Coated Tablet Comprising Sumatriptan The present invention provides a pharmaceutical composition for oral administration, comprising a core of active ingredient and an outer non-active layer formed on the core by application of pressure.
CN101053602B Medicine for treating oral ulcer and its preparing method The invention discloses a medicine for treating mouth ulcer. The primary material of the medicine is saxifrage which can combine with other plants. Said other plants are selected from one or more paddy, pricklyash peel, corn mint, and blumea balsamifera Dc or their mixture. The weight ratio of the saxifrage to other plants is 1:100-100:1. The inventive medicine has a curative effect to the mouth off-flavor generated by mouth microbe community and traumatic ulcer, mouth ulcer generated by the virus or bacteria injury and also can be used for recrudescence mouth ulcer, lichen planus generated by unknown reasons and autoimmune.
WO2013045519A1 Derivatives of 6-substituted triazolopyridazines as rev-erb agonists The present invention provides novel 6-substituted [1,2,4]triazolo[4,3-b]pyridazines that are agonists of Rev-Erb. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the activation of Rev-Erb has therapeutic effects, for instance in inflammatory and circadian rhythm-related disorders or cardiometabolic diseases.
EP1408988B1 Compositions of orally administered nutritional supplements to repair articular cartilage Provided is a synergistic combination of nutritional supplements classified as Nutraceuticals and further combined with antioxidant vitamins and minerals that, when orally administered to mammals, provides optimal delivery of vital metabolic precursors necessary for the production and repair of articular cartilage. Specifically provided is, a unique combination of chondroitin sulfate sodium, methylsulfonylmethane, glucosamine potassium, glucosamine hydrochloride, glucosamine sulfate sodium, N-acetyl D-Glucosamine, sodium absorbate and chelated manganese proteinate compounded through agitation. The provided compositions and methods of administration are designed to effectively elevate and sustain blood levels of said compounds in turn enhancing the body's natural chondroprotective mechanisms while providing an efficient delivery mechanism which optimizes cellular uptake of glucosamine and chondroitin. This process of forming specified synergistic relationships between vital metabolic precursors increases the body's production of proteoglycans, chondrocytes, hyalauron glycosaminoglycans and collagen, facilitating the repair and regeneration of articular cartilage and symptomatic relief from pain and inflammation associated with articular degeneration.
DE102006050511A1 New substituted dihydrotriazolone compounds are hypoxia-inducible transcription factor-prolyl-4-hydroxylase inhibitors useful to treat or prophylaxis e.g. heart insufficiency, anemia, chronic kidney diseases and renal failure Substituted dihydrotriazolone compounds (I) and their salts, solvates and solvates of the salts, are new. Substituted dihydrotriazolone compounds of formula (I) and their salts, solvates and solvate of the salts, are new. R1>, R2>nitrogen-containing heteroaryl group. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) the preparation of (I); and (2) a medicament comprising (I) in combination with an inert, non-toxic, pharmaceutical auxiliary material. [Image] - ACTIVITY : Cardiovascular-Gen; Cardiant; Antianemic; Antidiabetic; Vasotropic; Nephrotropic; Neuroprotective; Endocrine-Gen; Anabolic; Ophthalmological; Antiparkinsonian; Nootropic; Analgesic; Vulnerary; Cytostatic; Antianginal; Cerebroprotective; Antiarteriosclerotic; Hypotensive; Antimicrobial; Antiinflammatory; Gastrointestinal-Gen.; Antiarthritic; Antirheumatic. - MECHANISM OF ACTION : Hypoxia-inducible transcription factor-prolyl-4-hydroxylase inhibitor. Tests details are described but no results given.
WO2010089127A1 Substituted spiro-amides as b1r modulators The invention relates to substituted spiro-amides, methods for the production thereof, medicaments containing said compounds, and the use of substituted spiro-amides for producing medicaments.
EP2120946A1 Pharmaceutical composition comprising nicotinamide or nicotinic acid The present invention is directed to a pharmaceutical composition for oral administration containing nicotinamide/nicotinic acid as an active ingredient, as well as to the use of this pharmaceutical composition for the treatment of hyperphosphatemia.
US20090232888 Sustained delivery of antibiotics The present invention is directed to compositions for the sustained delivery of an antibiotic, for example vancomycin, to achieve desirable release profiles. This application is also directed to methods of using the compositions and processes for manufacturing the compositions.
US20120064025 Quinazolinone Modulators Of Nuclear Receptors Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.
EP1783120B1 Method of obtaining 2-amino-6-alkyl-amino-4,5,6,7-tetrahydrobenzothiazoles The invention relates to a method of preparing 2-amino-6-alkyl-amino-4,5,6,7-tetrahydrobenzothiazoles having formula (I), wherein the asterisk (*) represents an asymmetrical carbon and R1 is alkyl C1-C6, the enantiomers or mixtures thereof, the pharmaceutically-acceptable solvates, hydrates or salts of same. The inventive method comprises the following steps consisting in: (a) reacting a compound (II) with a secondary amine, optionally in the presence of an acid and a solvent 1, in order to form an enamine; (b) optionally removing the acid and solvent 1 and, subsequently, reacting the enamine with sulphur in the presence of a solvent 2; and (c) reacting the previously obtained compound with cyanamide in order to obtain compound (I). Compounds having formula (I) include pramipexol which is a compound with dopamine D2 agonist activity that can be used for the treatment of Parkinson's disease and schizophrenia.
WO2012021800A3 Caspase inhibitors as therapeutics for neural and organ injury and imaging Compounds, pharmaceutically acceptable salts thereof, and compositions useful as caspase inhibitors are disclosed. Certain compounds are also useful for the treatment of neural or organ injury. Other compounds are useful as neural and organ-specific imaging agents.
WO2009081970A1 Process for production of heterocycle-substituted pyridine derivative Disclosed is a process for efficiently producing a heterocycle-substituted pyridine derivative. Specifically disclosed is a process for producing a compound represented by Formula (I), which comprises the step of reacting a compound represented by Formula (III) with a compound represented by Formula (II) in a solvent in the presence of a Pd catalyst and a base. In Formulae (I) to (III), R1 represents a hydrogen atom or the like; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group which may be protected by a protective group or the like; one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom; Q represents a leaving group; the ring A represents a 5- or 6-membered heteroaryl or benzene ring which may have one or two halogen atoms or C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom or the like; R represents a hydrogen atom, a C1-6 alkyl group or the like; R3 represents a hydrogen atom, a halogen atom or the like; and R4 represents a hydrogen atom or a halogen atom, provided that all of R1, R2 and R4 do not represent a hydrogen atom when Z represents a single bond or when R3 represents a hydrogen atom.
US20120149721 Methylpyrrolopyrimidinecarboxamides The compounds of Formula (I), wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
CN1660432A Preparation of compound Tatin class and hepatic protectant and applications A medicine contains proportionally tatin medicine, liver-protecting medicine, skeleton and medicinal additive is disclosed. A packing box containing 60 tablets of tatin medicine and 60 tablets of liver-protecting medicine is also disclosed.
CN103006785A Chinese and western medicine compound transdermal solution and preparation method thereof The invention discloses a Chinese and western medicine compound transdermal solution and a preparation method thereof. The Chinese and western medicine compound transdermal solution comprises the components in percentage by weight as follows: 0.1%-5% of doramectin; 10%-50% of eucalyptus oil; 2%-3% of azone; 0.1%-2% of a stabilizing agent and 40%-50% of a diluting solvent. The preparation method for the Chinese and western medicine compound transdermal solution comprises the steps of heating eucalyptus oil; adding the stabilizing agent to form a stabilized eucalyptus oil solution; adding doramectin and azone, stirring and dissolving to form a reserved solution; adding the diluting solvent into the reserved solution to form the Chinese and western medicine compound transdermal solution. According to the Chinese and western medicine compound transdermal solution and the preparation method thereof, the compound transdermal solution provided by the invention can be directly rubbed at psoriasis part of a pet, namely psoriasis of the pet can be healed, so that the treatment process is simple, the operation is convenient, and the acarid and fungus killing effect is remarkable.
US7427418 Phloridzin-rich phenolic fraction and use thereof as a cosmetic, dietary or nutraceutical agent A phenolic fraction of fruit obtained from the Rosaceae family and also to the process for the specific extraction of this fraction. The phenolic fraction is rich in dihydrochalcones (phloridzin and phloretin) and may be used as a cosmetic, dietary, or nutraceutical preparation.
WO2010067335A1 Platinum (iv) complexes for use in the treatment of proliferative diseases such as cancer Provided are nitroplatinum(IV) complexes which may be useful treating various forms of proliferative diseases, such as cancer. In some instances the platinum(IV) complexes are relatively stable and may be suitable for oral administration. Also provided are methods of treatment, as well as kits and unit dosages.
EP1635833B1 Combination of opioids and a piperazine derivative for the treatment of pain This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1-(1,2-disubstituted piperidinyl)-4substituted piperazine derivatives having neurokinin antagonistic activity, in particular NKI antagonistic activity the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in acute and chronic pain treatments, more in particular in inflammatory, postoperative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NKI -receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression and tolerance in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise NK1- antagonists according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side-effects associated with opioid analgesics, in particular respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.
WO2009037542A3 Spirocyclic compounds as stearoyl coa desaturase inhibitors The present invention provides Stearoyl CoA Desaturase (SCD) inhibitors. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase 1 (SCDl). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase (SCD).
US7183251 hCG therapy for the treatment of breast cancer This invention relates to the field of cancer therapy. More particularly, the invention relates to the treatment of mammary tumor, clinically manifest mammary tumor (breast cancer) and metastatic mammary tumor by administration of human Chorionic Gonadotropin (hCG). The treatment preferably comprises the administration of hCG in conjunction with an antiestrogen and/or a Type I Interferon.
CN102973495A Method of slowing down degradation of sodium hyaluronate in body The invention relates to a method of slowing down degradation of sodium hyaluronate in a body. The method comprises adding a certain amount (0.5-30 micromoles per liter) of manganous chloride in ingredients of sodium hyaluronate injection. After viscoelastic material supplement therapy (injecting the sodium hyaluronate) is conducted in joints of an osteoarthritis patient, through supplementing exogenous sodium hyaluronate to recover the lubricating function of synovia, the recovery of cartilages can be promoted, and joint functions can be improved. However, the exogenous sodium hyaluronate stays in the joints for a short time, and compared with traditional sodium hyaluronate injection, the sodium hyaluronate injection containing the manganous chloride enables main gradients of the sodium hyaluronate to stay in the joints for a longer time, thereby improving treating effect and reducing treating cost of the patient.
CN101148463A Azithromycin derivative and application thereof The present invention discloses one kind of azithromycin derivative as shown and its pharmaceutically acceptable salt. The present invention also discloses the application of the azithromycin derivative in preparing medicine for preventing and treating bacterial infection diseases.
CN103110608A Entecavir capsules and preparation method thereof The invention discloses entecavir capsules and a preparation method thereof. The entecavir capsules are formed by uniformly mixing dry particles with talcum powder and filling the mixture to the capsules, wherein the dry particles are prepared by the following method: dissolving entecavir and a solid dispersion carrier in absolute ethyl alcohol; adding and uniformly dispersing a disintegrating agent which is insoluble in alcohol, and drying the solution under reduced pressure to remove absolute ethyl alcohol to obtain the solid dispersion which is adhered to the surface of the disintegrating agent; and carrying out wet-process pelletizing to the solid dispersion, a filling agent and a binding agent and drying to obtain the dry particles. According to the entecavir capsules and the preparation method thereof disclosed by the invention, the problem that the solid dispersion is unlikely to take out due to the viscosity is solved; and meanwhile, the dissolution rate of the product is greatly improved, the preparation process is relatively simple, convenient to operate and suitable for large-scale industrial production.
CN101390828B Anticancer composition loaded with anti-metabolism medicine and synergist thereof Disclosed is an anticancer combination which contains antimetabolics and the synergist thereof, and is a sustained-release injection. The anti-cancer combination is composed of sustained-release microspheres and solvent; wherein, the sustained-release microsphere contains effective anticancer ingredients and auxiliary material; the solvent is common solvent or special solvent which contains suspending agent. The viscosity of the suspending agent is 100cp-3000cp (20 DEG C-30 DEG C) and is selected from carboxymethyl cellulose; the antimetabolics is selected from methotrexate, fluorouracil, carmofur, tegafur, decitabine, capecitabine or gemcitabine; the synergist is tetrazine medicine or anticancer antibiotics; the auxiliary material is selected from p(LAEG-EOP), p(DAPG-EOP), or polyphosphate copolymer, or copolymer or mixture of polyphosphate, polylactic acid, polifeprosan, sebacic acid and PLGA; the anticancer combination also can be made into sustained-release implants which can be injected or implanted in tumor or the periphery of tumor with the effective medicine concentration maintained for more than 50 days; meanwhile, the systemic reaction of the medicine is obviously reduced; the treatment effects of the non-operative treatments such as chemotherapy or radiation treatment are selectively enhanced.
CN103520342A External medicine for treating scald and preparation method of external medicine The invention discloses an external medicine for treating scald and a preparation method of the external medicine. The external medicine is mainly prepared from gallnut, sanguisorba officinalis, Coptis chinensis, rheum officinale and golden cypress in a certain weight ratio. The medicine has the functions of promoting blood circulation, removing blood stasis, removing heat, detoxifying, eliminating swelling and stopping pains, and is quick in effect and relapse-free when used for treating the scald.
CA2676977A1 Use of chromium histidinate for treatment of cardiometabolic disorders Provided herein are methods for treating, preventing, and improving conditions associated with cardiometabolic syndrome, by identifying a subject in need of treatment, prevention, or improvement of a condition associated with cardiometabolic syndrome, and providing a therapeutically effective amount of a composition comprising chromium and histidine, chromium histidinate complexes, or combinations thereof, to the individual.
CN102614147A Slow release tablet containing quetiapine fumarate The invention discloses a slow release tablet containing quetiapine fumarate. The quetiapine fumarate slow release tablet mainly comprises quetiapine fumarate, modified pregelatinized starch, a filling agent, a bonding agent and a lubricating agent, wherein the mass ratio of the quetiapine fumarate in terms of quetiapine to the modified pregelatinized starch to the filling agent to the bonding agent to the lubricating agent is 1:(0.5-2):(0-1):(0.02-0.25):(0.01-0.5). The quetiapine fumarate slow release tablet prepared with the method can be used for treating schizophrenia. The product has the advantages of reduction in administration times, improvement on the taking compliance of patients, enhancement on the medicament effect and administration safety, and the like, and is more suitable for patients to use. Meanwhile, the slow release tablet has a simple process, and contributes to industrial mass production.
EP1179344B1 Release-regulating preparations Medicinal compositions which contain at least one member selected from among compounds represented by general formula (I), salts of these compounds, solvates of these compounds and solvates of these salts, and can reduce contact of such a compound with components of bile or pancreatic juice.
WO2005095356A1 Agent for generating heat or singlet oxygen and composition for cancer treatment each comprising organic peroxide or chemiluminescent compound An agent for heat generation or singlet oxygen generation which, unlike anticancer agents of the alkylating agent type such as MMC, destroys cancer cells by the action of heat and/or singlet oxygen and is effective as a new cancer remedy alleviating the burden to be imposed on the patient. The heat and/or singlet oxygen generator or cancer remedy comprises an organic peroxide, e.g., a peroxide of an imidazole derivative, or a chemiluminescnet compound, e.g., a dioxcetane compound.
CN101381418B Sterculia seed single polysaccharide SPA, preparation method and application thereof The invention discloses single polysaccharide SPA for boat-fruited sterculia seed and a preparation method thereof. The SPA mainly comprises the following components in percentage by weigh: 17 to 18 percent of pectinose, 11 to 12 percent of rhamnose, 15 to 16 percent of galactose, 0.5 to 1 percent of xylose, 0.1 to 0.5 percent of glucose, 39 to 40 percent of galacturonic acid, and 1 to 2 percent of glucuronic acid (mass percentage), and the weight average molecular weight of the SPA is 1.125x10<6>Da. The preparation method comprises the steps of separating and purifying the SPA from crude polysaccharide which is subjected to water extraction and alcohol precipitation after ultrasonic treatment and preliminary purifications such as deproteinization and so on, by adopting a CTAB precipitation method. The SPA has better inhibitory activity to acute inflammations, swelling as well as acute and chronic inflammations such as chronic granulo matosis and so on.
US20070259037 Method and composition for treatment of inflammatory conditions Methods of treating inflammation of the gastrointestinal tract and/or systemic or local inflammation by administering a steroid anti-inflammatory or a non-steroid anti-inflammatory drug in conjunction with polyunsaturated fatty acids or their derivatives and optionally also a pharmacologically active antioxidant and compositions for practicing these methods are described.
EP2421532A2 Spiperone derivatives and methods of treating disorders Described herein are spiperone derivative compounds which have been found to be useful in methods of stimulating CaCC and treating disorders (or symptoms thereof) associated with CaCC including cystic fibrosis, wherein a compound of the invention is administered to a subject.
WO2006068166A1 Dry granulated substance and process for producing the same Dry granulation of a mixed powder with high drug content has been accompanied by in the event of poor fluidity of medicinal agent, failure to appropriately feed powder to a machine for compression molding, and accompanied by in the event of extremely poor compression moldability of medicinal agent, difficulty in obtaining a molded form. There is provided a process comprising adding to an ingredient with medicinal effect (1) light anhydrous silicic acid and (2) a low-melting-point substance being solid at ordinary temperature and carrying out dry granulation of the mixture. By virtue of the process, excellent fluidity can be ensured without being influenced by the properties of drug, and after dry granulation, there can be obtained a dry granulated substance maintaining high compression moldability and, through tableting of the dry granulated substance, a tablet.
WO2012058993A1 Use of ambrisentan for preventing or alleviating cardiac function injury caused by hypoxia A use of ambrisentan or pharmaceutically acceptable salts thereof for preparing medicines for preventing or alleviating cardiac function injury or secondary diseases thereof caused by hypoxia, said secondary diseases being selected from right ventricular hypertrophy, pulmonary hypertension, vascular proliferation, pulmonary artery blood vessel thickening, pulmonary oedema and respiratory failure.
US20100247640 Solid Oral Dosage Form Containing An Enhancer The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.
CA2066384C Gastrointestinal mucosa-adherent matrixes, pharmaceutical preparation and a coating composition A solid matrix composition which is solid at ambient temperature, which comprises a viscogenic agent, such as an acrylic acid polymer, capable of developing viscosity on contact with water, as dispersed at least in the neighborhood of the surface layer of a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient. The matrix may be such that a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient has been coated with a coating composition containing at least one viscogenic agent. Such composition can adhere to the digestive tract and remain there for a prolonged period of time, thereby increasing the bioavailability of the active ingredient. Solid preparations, such as fine granules and granules, contain the above matrix composition.
WO2005099759A1 Medicine for prevention and/or treatment of arteriosclerosis A medicine for prevention and/or treatment of arteriosclerosis and diseases associated therewith, comprising as active ingredients a substance having the efficacy of retinoid X receptor (RXR) activation (for example, 4-[2,3-(2,5-dimethyl-2,5-hexano)dibenzo[b,f][1,4]thiazepin-11-yl]benzoic acid or 2-[N-cyclopropylmethyl-N-(5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalen-2-yl)amino]pyrimidine-5-carboxylic acid, etc.) and a substance having the efficacy of activating peroxisome proliferator-activated receptor Ϝ (PPARϜ) (for example, troglitazone or rosiglitazone, etc.).
CN1872039A Rotula of acetaminopher suitable for children to take, and prepartion method A sweet pill of acetylaminophenol is disclosed, which is suitable for children. Its preparing process is also disclosed.
EP2268140A2 Novel compounds advantageous in the treatment of central nervous system diseases and disorders A series of novel compounds showing anticonvulsant activity is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system ("CNS") diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.
US8017607 N-substituted-pyrrolidines as inhibitors of MDM2-P-53 interactions There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.
CN102380102A Method for preparing environment-responsive mesoporous silicon nanoparticles The invention relates to a method for preparing environment-responsive mesoporous silicon nanoparticles. The mesoporous silicon nanoparticles with the particle size of 20 to 1,000nm, the pore size of 2 to 50nm, the specific surface area of 500 to 1,500m<2>/g and a controlled structure are prepared by a template extraction method and subjected to surface functionalization by a self-assembly technology. A medicine sustained-release system prepared by the method is high in biocompatibility and medicine loading rate, can be released intelligently and controllably and has good application prospects in fields of growth factor and gene release, enzyme immobilization, cancer treatment and the like in tissue engineering, the preparation method is simple, reaction conditions are mild, and experiment raw materials are low in cost.
CN1623560A Preparation method of antiadhesion protective preparation A process for preparing the anti-adhesion protector with high adhesion, tissue affinity and bacterial suppression for preventing the adhesion between organs and hemorrhage includes such steps as proportionally mixing erucic acid with carboxymethyl cellulose sodium, stirring, adding acenocoumarol and adrenine, stirring, adding dihydrated terramycin, and stirring.
CN102813658A Composition of cefazolin sodium pentahydrate and tazobactam sodium or tazobactam sodium hydrate The invention relates to a composition of cefazolin sodium pentahydrate and tazobactam sodium or tazobactam sodium hydrate. Compared with the antibacterial effect of cefazolin sodium pentahydrate cefazolin sodium, the composition has excellent antibiotic activity and low resistant rates.
CN102631504A Medicine composition for treating white vein disease and preparation method of medicine composition The invention relates to a medicine composition for treating a white vein disease and a preparation method of the medicine composition. A process for ershiwuwei shanhu wan is improved, and twenty five medicines are crushed into micro-powder with the size ranging from 0.1 micrometer to 50 micrometers to form the medicine composition. The invention further relates to a preparation containing the medicine composition. Experiments show that the medicine composition resolves difficult process problems that surfaces of traditional pills are rough, differences of the pills are large, disintegration is poor, moisture and microorganisms exceed standards and the like, the production cycle of the preparation is shortened, cost is relatively low, industrialization and mechanization degrees are high, and the medicine composition meets requirements of modern pharmaceutical technology and regulations, and is convenient in use and more excellent in curative effect.
US6943179 Biurethane derivatives Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumors
CN1762350A Bendazac lysine eye drops with reduced irritability, its preparation method and application The invention discloses a bendazac lysine eye drops with reduced irritability, its preparation method and application, wherein the eye drop is prepared from bendazac lysine, thickening agent, buffering agent, preservative agent, isotonic agent, substance for reducing eye drop pungency and water for injection.
CN101732261B Stable type compound pellet, preparation method thereof and capsule containing same The invention discloses a stable type compound pellet, a preparation method thereof and a capsule containing the same. The stable type compound pellet is provided with a film coating layer, a main medicine layer, an isolation layer and a pill core from the outside to the inside. The main medicine layer is positioned between the film coating layer and the isolation layer, and the pill core is sealed in the isolation layer. The medicinal effective component of the main medicine layer is vitamin B12, and the mass of the vitamin B12 is 3-10% of the mass of the total solid of the main medicine layer. The medicinal effective components of the pill core are vitamin B1 and vitamin B6, and the mass ratio of the vitamin B1 to the vitamin B6 is 1:0.5-2 (W/W). The stable type compound pellet is prepared by adopting the procedures of pelletizing and coating. At a storage state, the vitamin B12 can not contact with the vitamin B1 and the vitamin B6 in the pill core, thereby avoiding the degradationof medicinal components because of mutual reactions and prolonging the storage time limit.
EP1165576B1 Process for preparing amine platinum complexes The present invention relates to the area of platinum drugs. In particular, it relates to an improved process for preparing platinum complexes having general formula (Ia) or (Ib), comprising: 1a) a first step, wherein [PtA4]2- is reacted with L under appropriate conditions in a first solvent to form [PtA¿3(L)]?-; 1b) a second step, wherein [PtA¿3(L)]?- is reacted with L' under appropriate conditions in a second solvent to form cis-[(PtA¿2?(L')(L)]; 1c) in the case there Y is halogen or hydroxy a thrid step, wherein cis-[PtA?2¿(L')(L)] is reacted with H¿2?O2, Y2 or halogen containing oxidant to form c,t,c-[PtA2Y2(L')(L)]; in the case where Y is carboxylate, carbamate or carbonate ester a fourth step, wherein an intermediate, where Y is hydroxy formed in step 1c), is functionalized with an appropriate acylating agent; and 1d) in the case where A is not a halide or is different from the original halide, additional step(s) in which the original halide A of an intermediate formed in step 1a or 1b, 1c or 1d is converted to a different halide or a new leaving group(s) A such as mono-dentate hydroxy, alkoxy, carboxylate or bi-dentate carboxylate, phosphonocarboxylate, diphosphonate, or sulphate; wherein L L' and Y have the meaning as defined in the description.
US20100298358 Naphthamide Derivatives As Multi-Target Protein Kinase Inhibitors and Histone Deacetylase Inhibitors Isolated compounds of formula I: and stereoisomers, enantiomers, diastereomers, and pharmaceutically acceptable salts thereof are described, as well as processes for production, and methods of use of these compounds and compositions thereof for the treatment of diseases associated with abnormal protein kinase activities and/or abnormal histone deacetylase activities including, for example, inflammatory diseases, autoimmune diseases, cancer, neurological and neurodegenerative diseases, cardiovascular diseases, metabolic disease, allergies and asthma and/or hormone-related diseases.
CN101991592A Application of paederoside to preparation of analgesic and/or anti-inflammatory medicaments The invention provides application of paederoside to the preparation of analgesic and/or anti-inflammatory medicaments. The paederoside provided by the invention has good effect on peripheral analgesia and central nervous analgesia and has good anti-inflammatory effect at the same time, so that the paederoside can be used alone or used in coordination with other pharmaceutically available components to prepare the analgesic and/or anti-inflammatory medicaments.
WO2013073483A9 Method for producing myo-inositol and myo-inositol derivative [Problem] To impart significantly improved myo-inositol producing capability, suitable for use in recombinant DNA techniques and synthetic biology methods, to a host microorganism that does not possess an endogenous myo-inositol biosynthesis pathway, such as Escherichia coli. [Solution] Inositol monophosphatase activity is strengthened in a transformant obtained by introducing a myo-inositol biosynthesis pathway into a host microorganism that does not possess an endogenous myo-inositol biosynthesis pathway.
EP2167508A1 Compounds for treating duchenne muscular dystrophy Compounds of general formula (I), wherein X1, X2, X3, R1, R2, R3, Y and Z are as defined herein are useful for the treatment and prevention of Duchenne muscular dystrophy, Becker muscular dystrophy and cachexia.
US20100222439 Beverage containing a polymeric polyphenol This invention relates to a polymeric polyphenol containing beverage, In particular it relates to a substantially clear ambient temperature beverage comprising tea solids derived from fermented tea. The invention also relates to a method for improving the clarity of a polymeric polyphenol containing liquid composition. It has long been observed that on cooling an aqueous black tea infusion from about 90 degrees Celsius to ambient temperature, a marked increase in the turbidity of the infusion can be seen leading ultimately to precipitation of up to about 30% w/w of the total tea solids. This precipitate is known as tea cream. It is thought that this precipitate originates from initial self-associations of polymeric polyphenols and association with caffeine thereby forming nano-clusters. These nano-clusters are not themselves responsible for any turbidity or precipitation of tea solids. However as the solubility of the polymeric polyphenols further reduces on cooling of the aqueous black tea infusion, these nano-clusters then aggregate into larger sub-micelles and ever larger micelles which are responsible for the turbidity and precipitate. A solution to the aforementioned problem is provided in a first aspect of the invention by a beverage comprising tea solids, a liquid vehicle, added protein and added anionic polysaccharide, wherein the beverage has a cream inhibition (CI) of 70-100%, preferably 80-100%, wherein CI=(1−((ODS−ODB)/(ODO−ODB)))100 where ODS is the optical density of the beverage, ODB is the optical density of the tea solids in a 25% w/w aqueous solution of ethanol and ODO is the optical density of the beverage but in the absence of the protein and anionic polysaccharide additional to any in the tea solids, the optical density being measured at a fixed path length at 600 nm and at 4 degrees Celsius after equilibration at 4 degrees Celsius for 24 hours.
US20100331349 Use of gamma-aminobutyric acid to mask or reduce an unpleasant flavour impression and preparations containing gamma-aminobutyric The use of γ-aminobutyric acid or a physiologically acceptable salt of γ-aminobutyric acid to mask or reduce the unpleasant flavour impression of an unpleasantly tasting substance is described. The food, beverage or oral care preparations or oral pharmaceutical preparations comprising at least one unpleasantly tasting substance and γ-aminobutyric acid are also described.
CN103536558A Cefoperazone sodium composition freeze-dried powder for injection The invention provides a cefoperazone sodium composition freeze-dried powder for injection, and belongs to the field of medicine and medicine preparation technology. The cefoperazone sodium composition freeze-dried powder comprises following raw material ingredients, by weight, 7.26 to 9.17 parts of cefoperazone sodium, 4.36 to 5.50 parts of chitosan nanoparticle, and 84.38 to 89.10 parts of injection water. Advantages of the cefoperazone sodium composition freeze-dried powder are that: 1) antibacterial activity of the cefoperazone sodium composition is increased significantly; 2) antibacterial spectrum is widened, and drug tolerance is reduced greatly; 3) improvement of activity is capable of shortening medication cycle of patients, and reducing occurrence likelihood of adverse reaction caused by accumulation of cefoperazone sodium; and 4) the chitosan nanoparticle can be used as a freeze-dried skeleton agent of the freeze-dried powder injection instead of mannitol, so that active effects of mannitol on human bodies are avoided.
WO2010009809A3 Active substance combinations consisting of an anis fruit extract and hyaluronic acid The invention relates to active substance combinations consisting of an effective amount of anis fruit extract and hyaluronic acid.
CN101822837A Medicine composition containing allisartan isoproxil salts The invention relates to a medicine composition containing pharmaceutically acceptable salts containing allisartan isoproxil, at least one cardiovascular and cerebrovascular medicine and pharmaceutically acceptable vectors. The composition is used for preventing, slowing the progress of or treating the following diseases or symptoms of: hypertension, hypertension complications, diabetes, diabetes complications, dyslipidemia, ischemic diseases, coronary heart disease, angina, cardiac arrhythmia, stroke, arteriosclerosis, cerebral infarction, cerebral vascular diseases, cardiovascular diseases, coronary artery diseases, ventricular dysfunction, endothelial dysfunction, heart insufficiency, glaucoma and cataract, reducing the incidence and/or the mortality of cardiovascular and cerebrovascular diseases, decreasing the side effects, and also improving the medication compliance of patients.
CA2178605C Pharmaceutical formulation for preventing or pre-treating poisoning by organophosphoric cholinesterase inhibitors A pharmaceutical formulation for preventing or pre-treating poisoning by organophosphoric cholinesterase inhibitors is characterized in that it consists of an active substance combination of at least one parasympathomimetic agent and at least oneparasympatholytic agent.
CN101219102A Lapatinib sustained-release implantation agent for treating solid tumors The invention relates to a solid tumors-curing Lapatinib sustained-release implant, which is characterized in that the sustained-release implant contains effective anti-tumor dose of Lapatinib, sustained-release auxiliary material and a certain amount of sustained-release regulator. Solid tumors consist of lung cancer, esophageal cancer, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic cancer, bladder cancer and colorectal cancer. The sustained-release auxiliary materials are mainly one or mixture of copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co-propyl phosphate). When the sustained-release auxiliary materials are degrading and absorbed, Lapatinib is slowly released into tumor part, thus while reducing toxic reaction of the whole body, the sustained-release auxiliary materials can sustain concentration of effective drug at the tumor part. Placing the anti-tumor sustained-release implant at the tumor part can not only reduce toxic reaction of the whole body of Lapatinib, but also improve drug concentration at the tumor part and enhance treatment effects of nonspecific treatments, such as chemotherapeutics, radiotherapy, etc.
EP1343495B1 Methods of treating anxiety disorders This invention provides methods for treating, preventing or inhibiting anxiety, anxiety-related conditions and phobias in a mammal using compounds of the formula (I) wherein: R1 is H, alkyl, alkanoyl or the radical Ar; R2 is H or alkyl; R3 is alkoxy, NH2, alkylamino, dialkylamino, amino substituted by the radical Ar, alkyl, alkenyl, alkynyl, or the radicals Ar or ArO-; R4 is H, alkyl or the radical Ar; R5 is H or alkyl or the radical Ar; or a pharmaceutically acceptable salt or ester form thereof; Ar is an optionally substituted phenyl radical; and n is O or 1, or a pharmaceutically acceptable salt or ester form thereof, with the methods particularly including the use of N-[2-amino-4-(4-fluorobenzylamino)-phenyl]carbamic acid ethyl ester, also known as retigabine.
WO2011112434A1 Compositions and methods for producing consumables for patients with dysphagia Compositions are provided that are suitable for safe consumption by a patient with dysphagia. In one embodiment, the compositions include a modified xanthan gum in an amount suitable to provide a viscous, free-flowing solution having gel-like properties. The modified xanthan gum comprises a non-pyruvylated xanthan gum, a reduced-pyruvylated xanthan gum, or a combination thereof. The composition desirably has a viscosity of greater than about 2000 cP and is characterized as having a shape retention of greater than about 50%. Also provided are methods for their preparation and use.
US20070297981 Formulations and methods for treating dry eye The present invention provides compositions for treating and/or preventing signs and symptoms associated with dry eye and/or ocular irritation, and methods of use thereof. Such compositions are provided in novel ophthalmic formulations that are comfortable upon instillation in the eye.
EP0951292B1 Treating an ischemic disorder and improving stroke outcome The present invention provides for a method for treating an ischemic disorder in a subject with comprises administering to the subjet a pharmaceutically acceptable form of a selection antagonist in a sufficient amount over a sufficient time period to prevent white blood cell accumulation so as to treat the ischemic disorder in the subject. The invention further provides a method for treating an ischemic disorder in a subject which comprises administering to the subject carbon monoxide gas in a sufficient amount over a sufficient period of time thereby treating the ischemic disorder in the subject. The invention further provides a method for treating an ischemic disorder in a subject which comprises administering to the subject a pharmaceutically acceptable form of inactivated Factor IX in a sufficient amount over a sufficient period of time to inhibit coagulation so as to treat the ischemic disorder in the subject.
CN100584326C Function of stilbene oxygen acid or salt in preparing antiatheroscloresis medicament The invention relates to stilbene oxo acid compound of type (I) and a new application of the type (I) that the acceptable salt is used to prepare the hypolipidemic drugs in pharmacy. Wherein, R1 is H, CH2COOH or C(CH3)2COOH; R2 is H, CH2COOH, C(CH3) 2COOH or glucosyl; R3 is H, CH2 COOH or C(CH3)2COOH; and when the R1 and R3 are different, the type (I) is H. The hypolipidemics refers to reducing serum triglyceride, total cholesterol, and reducing the level of LDL cholesterol and increasing the level of HDL cholesterol. The hypolipidemic drugs are drugs which are used to treat and/or prevent diseases such as hyperlipidemia, high cholesterol, fatty liver and anti-atherosclerosis, etc. in clinical practice.
EP2520292A1 Use of spirangiens for the treatment or prevention of IL-8 or IL-6 mediated disorders The invention relates to spirangien for use in the treatment or prevention of an Interleukin 6 (IL-6) or Interleukin 8 (IL-8) mediated disorder. The invention also provides a pharmaceutical formulation for use in the treatment or prevention of an IL-6 or IL-8 mediated disorder and a method of preventing or treating an IL-6 or IL-8 mediated disorder.
US7390924 Terphenyl derivatives, preparation thereof, compositions containing same The invention relates to terphenyl derivatives of formula: and to their preparation and to the pharmaceutical compositions comprising them. These compounds exhibit an antagonist activity with respect to CB1 cannabinoid receptors.
CN101390823A Medical composition containing quetiapine The invention discloses a medicinal combination which contains quetiapine and is composed of active ingredient quetiapine or other medicinal salt, medicinal stabilizer and medicinal auxiliary material. The medicinal combination is used for the clinical treatment of depressions correlated with biphasic psychotic disorders.
CN103130803A Oxidized iso-aporphine alkaloid derivative, synthetic method and application The invention discloses a new oxidized iso-aporphine alkaloid derivative-4,6-dis-(2-pyridyl)-5,6-dihydro-4H-1,5-diaza-benzo[de]cyclopentane[b]-8-anthranone(PPCA for short), a synthetic method and an application. The PPCA synthetic method comprises the following steps: weighting 1-nitrogen-5-bromobenzanthrone and 2-(aminomethyl)pyridine, taking 1-nitrogen-5-bromobenzanthrone for dissolving in n-amyl alcohol, adding the weighted 2-(aminomethyl)pyridine and performing backflow reaction at the temperature of 140-180 DEG C, cooling, performing pumping filtration, washing the filter residue, and drying to obtain the oxidized iso-aporphine alkaloid derivative. The invention investigates the oxidized iso-aporphine alkaloid derivative has inhibition activity on the propagation of various human tumor cell strains such as HepG2, MGC80-3, SK-OV-3 and T-24, the result shows that the oxidized iso-aporphine alkaloid derivative has obvious external antineoplastic activity and has good latent medicinal value. A structural formula of PPCA is shown in a following formula.
CN102188460A Medicament for treating psoriasis and its manufacturing method The invention relates to a medicament for treating psoriasis and its manufacturing method, wherein the medicament is composed of sesame oil, sulphur and citric acid; and the manufacturing method comprises dissolving the above sulphur and citric acid by using liquid paraffin, filtering the dissolved solution through a 400-mesh gauze, and finally adding the filtrate into sesame oil with stirring. The medicament provided by the invention has definite therapeutic effect, and psoriasis is not easy to recur after being healed. The manufacturing method provided by the invention is simple with the raw material easily available, has good economic benefit, and is convenient for popularization and application.
US20050026956 Carbinols for the treatment of neuropathic dysfunction Compositions and methods are provided for treating neuropathic pain or neuropathic dysfunction that include the administration of an effective amount of a defined carbinol or a pharmaceutically acceptable salt or prodrug thereof.
US20130012513 Hedgehog inhibitors Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary disease and disorders.
CN103393624A Montelukast sodium membrane-shape preparation The invention discloses a Montelukast sodium membrane-shape preparation, which comprises a strip membrane band and a treatment effective dosage of active medicament Montelukast sodium loaded on the strip membrane band. The strip membrane band comprises an acidic strip membrane band and an alkaline strip membrane band, which are connected into a whole and mutually isolated; the acidic strip membrane band employs a high water-soluble polymer film forming material as a main body and comprises 1-20% of an acidizer, calculated by the weight of the membrane band; and the alkaline strip membrane band employs a high water-soluble polymer film forming material as a main body and comprises 1-20% of an alkaline agent, calculated by the weight of the membrane band. After encountering water, the preparation provided by the invention becomes an effervescent membrane and generates a large quantity of bubbles, so as to paralyze olfaction to cover smell and accelerate dissolution.
WO2009080351A1 Compounds with anti-emetic effect The present invention relates to the use of Melanocortin-4 receptor antagonists in the treatment of emesis and nausea.
CA2805265A1 Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina) The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of CTNNB1 gene expression and/or activity, and/or modulate a beta-catenin gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against CTNNB1 gene expression.
US20120114752 Stable tablet containing 4,5-epoxymorphinan derivative The present invention relates to a stable tablet comprising a 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt thereof as an effective ingredient. That is, the tablet according to the present invention comprises: (1) as the effective ingredient, a specific 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt; (2) sodium thiosulfate; (3) at least one selected from the group consisting of saccharides and sugar alcohols; and (4) crospovidone, sodium carboxymethyl starch or a mixture thereof, in which tablet the content of the aforementioned (4) is 1 to 20% by weight per unit weight containing the aforementioned effective ingredient.
US6900244 Controlling lipid, cholesterol metabolism; anticholesterol agents The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.
US20060275284 Combination therapy for treatment of autoimmune diseases using b-cell depleting/immunoregulatory antibody combination The present invention concerns treatment of autoimmune diseases with the combination of an immunoregulatory antibody, e.g. an anti-B7.1 or anti-B7.2 or anti-CD40L antibody and at least one B cell depleting antibody, such as CD19, CD20, CD22, CD23, or CD37, wherein such antibodies may be administered separately, or in combination, and in either order, over prolonged periods of time.
CN1769273A Meglumine glycididazole and its preparation method and uses as synergist of radiochemical therapy The invention relates to a meglumine glycididazole and its preparation method and uses as synergist of radiochemical therapy, wherein the preparing process comprises fully mixing and contacting aminoacetic diazole acid with meglumine in liquid environment to produce the salt with good water-solubility.
EP1750653A1 Use of heat shock protein inhibitorsfor the reduction of hair growth Mammalian hair growth is reduced by topically applying composition including a heat shock protein inhibitor.
WO2012060738A1 CLATHRATE COMPLEXES OF β-CYCLODEXTRIN WITH 1-{[6-BROMO-1-METHYL-5-METHOXY-2-PHENYLTHIOMETHYL-1-H-INDOLE-3-YL]CARBONYL}-4-BENZYLPIPERAZINE HAVING ANTIVIRAL ACTIVITY, THE PRODUCTION AND USE THEREOF The invention relates to a novel clathrate complex of β-cyclodextrin with 1-{[6-bromo-1-methyl-5-methoxy-2-phenylthiomethyl-1-H-indole-3-yl]carbonyl}-4-benzylpiperazine of formula (1), wherein the molar ratio of 1-{[6-bromo-1-methyl-5-methoxy-2-phenylthiomethyl-1-H-indole-3-yl]carbonyl}-4-benzylpiperazine derivatives : β-cyclodextrin is from 1 : 1 to 1 : 10. The invention also describes solid-phase and liquid-phase methods for producing and using the aforesaid clathrate complex.
CN102784116A High-dissolution fenofibrate dispersible tablet and preparation process thereof The invention discloses a high-dissolution fenofibrate dispersible tablet and a preparation process thereof. The dispersible tablet contains a main medicine, a filling agent, a disintegrating agent, a solubilizer, a lubricant and a proper amount of a binder. The preparation process provided by the invention is simple; the prepared dispersible tablet can rapidly disintegrate and uniformly disperse, is convenient to take and has a dissolution degree 20% higher than the dissolution degree of common tablets.
US20060229321 Rosuvastatin in pre demented states Provided is a method of preventing dementia in a patent comprising administering to a patient at risk of developing dementia an effective amount of rosuvastiatin or its pharmaceutically acceptable salt.
EP1824832A1 Aryl-substituted benzimidazole and imidazopyridine ethers as anti-cancer agents Aryl substituted benzimidazole and imidazo[4,5]Aryl substituted benzimidazole and imidazo[4,5]Aryl substituted benzimidazole and imidazo[4,5]pyridine ethers are described as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
CN103159650A Preparation and application of aromatic heterocyclic sulfonamide compound The invention relates to preparation and application of an aromatic heterocyclic sulfonamide compound, and in particular provides the aromatic heterocyclic sulfonamide compound. The compound is in a structure of the following general formula (I), the compound can effectively suppress survival and growth of SUM-159, HCC-1954 and MCF-7 cells, wherein n=0. 1, 2 or 3, and R is selected from C1-C4 straight chain or branched paraffin, phenyl, cyclohexyl, o-methylphenyl, 3- pyridyl and 2- pyridyl ethyl.
US20050033052 Pyrimidone compounds which are inhibitors of the enzyme Lp-PLA2; use in treating atheroscelerosis Pyrimidone and pyridone compounds of the formula: are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
CN103505476A Cell-free preparations of immunopotentiators, and preparation methods and uses thereof The invention relates to a cell-free preparation of a pseudomonas preparation, a cell-free preparation of a Bacillus Calmette-Guerin polysaccharide and nucleic acid preparation, a cell-free preparation of a Nocardia rubra cell wall skeleton preparation, a cell-free preparation of a Group A Streptococcus preparation, a cell-free preparation of a Pseudomonas aeruginosa preparation, and a cell-free preparation of a Brucella preparation. The above cell-free preparations have a granularity of 10-1000nm, preferably 10-800nm, and more preferably 10-500nm. The pyrogens of Gram-positive bacteria are below 320EU/ml, and preferably below 120EU/ml. The preparation methods of the cell-free preparations comprise the following steps: heating the preparations for boiling for 15-60min to obtain inactivated bacterial liquids; washing aseptic-test-qualified bacterial liquids, and breaking thalli under an aseptic condition by using a breaker; centrifuging a suspension obtained after breaking the thalli, collecting the above obtained precipitate, and washing the precipitate to prepare a suspension; and packaging the suspension, and carrying out heating disinfection to obtain the cell-free preparations of the preparations. The invention also relates to applications of the cell-free preparations.
US20120283213 Aryl/Alkyl Succinic Anhydride Hyaluronan Derivatives The present invention relates to the modification of hyaluronic acid (HA) with aryl/alkyl succinic anhydrides (ASA) to produce aryl/alkyl succinic anhydride HA derivatives, to the derivatives as such, and to their applications and uses, particularly in the cosmetic and biomedical industries. The ASA-HA derivatives are expected to have interesting properties that can be used for advanced formulation (bind stronger to the skin compared to non-modified HA), possibly also in delivery systems for actives or drugs by encapsulation (nano/micro capsules) or formation of nano/micro spheres. Further, the low MW ASA-HA derivatives are expected to penetrate the skin more efficiently than non-modified HA of the same MW.
CN103157108A An immunomodulator composition, and a pharmaceutical composition and applications thereof The present invention relates to an immunomodulator composition, and a pharmaceutical composition and applications thereof. The immunomodulator composition consists of a variety of bacterial polysaccharide extracts, wherein at least a bacterial polysaccharide extract derived from mycobacterium and a polysaccharide extract derived from pneumococcus are comprised. The immunomodulator composition can stimulate a body to produce a sustained immune function of a significant effect, particularly non-specific immune response ability as well as secondary generated specific immune response on the basis thereof. Compared with immunomodulators already available in the market, the immunomodulator composition of the invention can improve the overall anti-infection, anti-tumor and anti-allergic abilities for human or animals.
US20050107306 Treatment of respiratory disease associated with matrix metalloproteases by inhalation of synthetic matrix metalloprotease inhibitors The present invention encompasses methods and compositions for the treatment and prevention of respiratory diseases associated with matrix metalloproteases. More specifically, the present invention relates to the treatment and prevention of respiratory diseases associated with matrix metalloproteases by inhalation of synthetic matrix metalloprotease inhibitors. Exemplary respiratory diseases associated with matrix metalloproteases that may be treated by the methods of the invention include chronic obstructive pulmonary disease, emphysema, asthma, cystic fibrosis, and chronic bronchitis. An exemplary synthetic matrix metalloprotease useful in the methods of the invention is ilomastat.
CN1922157B Benzo[d]isoxazol-3-ol daao inhibitors Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: I wherein Z1 is N or CR3; Z2 is N or CR4; Z3 is O or S; A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2; R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl; at least one of R1, R2, R3 and R4 is other than hydrogen; and at least one of Z1 and Z2 is other than N.
WO2014016191A1 N-cyclopropyl-n-piperidinyl-amide derivatives and their use as gpr119 modulators The present invention relates to compounds of general formula I wherein R1 is selected from a group consisting of -CH2-Ra, wherein Ra denotes C1-6-alkyl optionally mono- or polysubstituted with fluorine, or C3-6- cycloalkyl optionally mono- or polysubstituted with fluorine and optionally substituted with a group selected from among CH3, CF3, and CHF2, and Lp, (Het)Ar1, (Het)Ar2 and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
CN1823813A Nursing and treating composition for female vagina and its preparation method A composition for nursing the vagina and treating the gynopathic inflammation such as vaginitis contains the chitosan or its cationic derivative (0.1-99 Wt%). Its preparing process is also disclosed.
WO2011031884A3 Methods and materials for modulating deubiquitinases and ubiquitinated polypeptides This document relates to methods and materials involved in modulating deubiquitinases (e.g., USP10 polypeptides) and/or ubiquitinated polypeptides (e.g., tumor suppressor polypeptides or mutant versions of tumor suppressor polypeptides). For example, methods and materials for increasing deubiquitinase (e.g., a USP10 polypeptide) expression or activity, methods and materials for decreasing deubiquitinase (e.g., a USP10 polypeptide) expression or activity, methods and materials for stabilizing tumor suppressor polypeptides (e.g., wild-type p53 polypeptides), methods and materials for de-stabilizing mutant versions of tumor suppressor polypeptides (e.g., mutant p53 polypeptides), and methods and materials for reducing cancer cell proliferation, increasing cancer cell apoptosis, and/or treating cancer (e.g., cancers having reduced levels of wild-type p53 polypeptides or cancers having increased levels of mutant p53 polypeptides) are provided. This document also provides methods and materials for identifying agonists or antagonists of USP10 polypeptide mediated stabilization of p53 polypeptides.
CN101040838A Anticancer compound including phosphatidylinositol 3-kinase inhibitor and alkylate The invention relates to an anti-cancer compound as a slow release injection which contains phosphoinositide 3-kinase restrainer and/or alkyl agent, formed by slow release micro ball and solvent. The slow release micro ball comprises the anti-cancer effective components and slow release findings selected from phosphoinositide 3-kinase restrainer and/or alkyl agent, the solvent is a common solvent or a special solvent with suspending agent, while the viscosity of suspending agent is 100cp-3000cp (at 20-30Deg. C), selected from carboxymethyl cellulose, the slow release finding is selected from phosphate polyester as p (LAEG-EOP), p (DAPG-EOP), p (BHET-EOP/TC), p (BHET-EOP/TC), p (BHDPT-EOP/TC), p (BHDPT-EOP/TC), p (CHDM-HOP) or p (CHDM-EOP), or the polyester or mixture of phosphate and polylactic acid, polyphenyl, 2-aliphatic acid, sebacic acid polyester, poly (erucic acid dimmer-sebacic acid) or poly (fumaric acid-sebacic acid). The anti-cancer compound can be made as slow release plant agent, to inject cancer or around cancer to hold the effective drug density for more than 60 days, while it can significantly reduce the general reaction of drug and selectively strengthen the effect of non-surgery treatments as chemotherapy or the like.
EP1153129B1 Method of treating restenosis by antisense targeting of c-myc The present invention provides an improved method for reducing the risk or severity of restenosis following cardiac angioplasty. The method includes administering to a target vessel region, a morpholino antisense compound having uncharged phosphorus-containing backbone linkages, and spanning the start codon of a human c-myc mRNA. Also disclosed are novel antisense compounds and compositions, and a method for assaying the effectiveness of antisense delivery and uptake to a target vessel region.
WO2007034200A1 2-aminoalcohols for the treatment of neurodegenerative diseases Use of a compound for the manufacture of a medicament for use in therapy of a neurodegenerative condition, wherein the compound is of formula (I): wherein R1 is CHR4-OR5 or CHR4-SR5, or aryl or heteroaryi optionally substituted with one or more groups R6; R2 is alkyl or is part of a ring with R3; R3 is H, alkyl or CH2 (when forming part of a ring with R2); R4 is H or alkyl or is part of a ring with R5; R5 is aryl or heteroaryi optionally substituted with R7; each R6 is independently alkyl, CF3, OH, Oalkyl, OCOalkyl, CONH2, CN, halogen, NH2, NO2, NHCHO, NHCONH2, NHSO2alkyl, CONH2, SOMe, SO2NH2, Salkyl, CH2S02alkyl or OCONalkyl2; R7 is R8 or (CH2)nOR8, R9, CF3, OH, OR9, OCOR9, COR9, COOR9, CONH2, CH2CONH2, CN, halogen, NH2, NO2, NHCHO, NHCONH2, NHCONHR7, NHCON(R9)2, NHCOR9, NHCOaryl, NHSO2Me, CONH2, SMe, SOMe or SO2NH2; R8 is (CH2)nOR9, (CH)nOR9, (CH2)nCOOR9or (CH2)nCOaryl; R9 is alkyl or cycloalkyl; and n is 1 to 4; or a salt thereof.
CN103656301A Application of Xinnaojia formula to preparation of liver protection medicine The invention discloses application of a Xinnaojia formula to preparation of a liver protection medicine. The key point of the technical scheme of the invention is the application of the Xinnaojia formula to the preparation of a medicine for treating liver injury caused by chronic alcoholism. The Xinnaojia formula has the benefits that the Xinnaojia formula has an excellent adjustment effect on lipid metabolism disorder caused by excessive alcohol consumption, and can improve liver function and blood fat to varying degrees.
CN1568968A Application of flavonol polyphenol in the preparing process of SARS treating medicine The invention discloses the use of pharmaceutical composition of flavonol polyphenol, in particular the pharmaceutical use of flavonol polyphenol in preparing medicament for treating or preventing Severe Acute Respiratory Syndrome (SARS).
US20120121527 NOVEL BIAROMATIC COMPOUNDS THAT MODULATE PPARy TYPE RECEPTORS AND COSMETIC/PHARMACEUTICAL COMPOSITIONS COMPRISED THEREOF Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.
US20080305142 Cell Free Biosynthesis of High-Quality Nucleic Acid and Uses Thereof The invention provides an improved cell free amplification method capable of producing large quantities of therapeutic-quality nucleic acids and methods of using the synthesized nucleic acid in research, therapeutic and other applications—The methods combine several different state-of-the-art procedures and coordinate their applications to affordably synthesize nucleic acids for therapeutic purposes. It combines in vitro rolling circle amplification, high fidelity polymerases, high affinity primers, and streamlined template specifically designed for particular applications. For expression purposes, the templates contain an expression cassette including a eukaryotic promoter, the coding sequence for the gene of interest, and a eukaryotic termination sequence. Following amplification, concatamers are subsequently processed according to their intended use and may include: restriction enzyme digestion for the production of short expression cassettes (SECs); ligation steps to circularize the SEC (CNAs); and/or supercoiling steps to produce sCNAs. The final product contains nearly non-detectable levels of bacterial endotoxin.
WO2003032894A3 Method of monitoring neuroprotective treatment Methods for monitoring and evaluating the efficacy of neuroprotective treatment of a patient suffering from neurological damage by measuring the amount of at least one biomarker in a biological sample taken from the patient during or after treatment.
EP1351688A4 Urotensin-ii receptor antagonists The present invention relates to a method of antagonizing the Urotensin-II receptor by 2-(NH-substituted) quinolones.
US8470812 Substituted benzo-pyrimido-tetrazolo-diazepine compounds The present invention relates to substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
WO2006053754A1 COMBINATIONS OF ANTI-ATHEROSCLEROTIC PEPTIDES AND AN mTOR INHIBITING AGENT AND THEIR METHODS OF USE The invention relates to a pharmaceutical compositions comprising a peptide which ranges in length from about 10 to about 30 amino acids, comprises at least one class A amphipathic helix and comprises at least one 'D' amino acid residue and an mTOR inhibiting agent, e.g. rapamycin or a rapamycin derivative, optionally in the presence of a pharmaceutically acceptable carrier.
US7625583 Microbiocidal fatty acids such as palmitoleic acid and lauric acid A source of dietary lipids containing anti-microbial fatty acids is added to a food composition intended for improving or maintaining the skin health and/or coat quality in a pet by preventing or regulating the growth of skin pathogens and of microflora responsible for the generation of body surface and coat odors.
US20100292650 Methods and Related Compositions for Reduction of Fat and Skin Tightening Compositions and methods useful in the reduction of localized fat deposits and tightening of loose skin in subjects in need thereof using pharmacologically active detergents are disclosed. The pharmacologically active detergent compositions can additionally include anti-inflammatory agents, analgesics, dispersion or anti-dispersion agents and pharmaceutically acceptable excipients. The pharmacologically active detergent compositions are useful for treating localized accumulations of fat including, for example, lower eyelid fat herniation, lipodystrophy and fat deposits associated with cellulite and do not require surgical procedures such as liposuction.
EP1311519A4 Thermosensitive cyclotriphosphazene-platinum complex conjugate, its preparation method and anticancer agent containing the same The present invention provides a novel thermosensitive cyclotriphosphazene-platinum complex conjugates represented by Formula (1) wherein m is a repeating unit of poly(alkoxyethylene glycol) selected from the integers 2, 7 and 12; n represents the length of the alkyl chain selected from the integers 0, 1, 2 and 3; x represents the length of the anionic amino acid residue selected from the integers 0 (amino malonic acid derivatives), 1 (aspartic acid derivatives) and 2 (glutamic acid derivatives); A2 is a bidentate chelating diamine selected from the group consisting of 2,2-dimethyl-1,3-propanediamine (dmpda), trans(+/-)-1,2-diaminocyclohexane (dach) and 1,1-diaminomethylcyclohexane (dmach).
CN101972442A Medicament for treating skin tinea The invention relates to a medicament for treating skin tinea. The medicament is prepared by mixing the following raw materials in part by weight: 0.1 to 5 parts of musk, 20 to 40 parts of purple paper garlic and 100 to 300 parts of white vinegar. The medicament has good curative effect of treating the skin tinea.
CA2335107C Leptin-mediated gene-induction Using the PC12 cell line as a model system a series of transcripts induced through activation of the leptin receptor or gp130 was identified. Based on kinetic studies on undifferentiated PC12 cells, two distinct gene-sets could be discerned: STAT-3, SOCS-3, Metallothionein-II, the serine/threonine kinase Fnk and the rat homologue of MRF-1 which are immediate early response genes, and Pancreatitis Associated Protein I, Squalene Epoxidase, Uridinediphosphate Glucuronyl Transferase and Annexin VIII, which are late induced target genes. In the latter case only, a strong co-stimulation with the adenylate cyclase activator forskolin was observed. Two additional transcripts encoding Leptin Induced Protein I(LIP-I) and Leptin Induced Protein II (LIP-II) were also identified. LIP-II is a rat orthologue of the human Down Syndrome Cell Adhesion Molecule (DS-CAM). In both cases, no forskolin co-stimulatory effect was observed. On PC12 cells differentiated to a neural phenotype by combined .beta.-NGF and forskolin treatment, Pancreatitis Associated Protein III, Peripherin and Mx2 protein were further identified as being regulated by leptin. Finally, from an RDA experiment using mRNA from either hyper-IL-6-or leptin-induced PC12 cells, the Reg gene, another member of the Pancreatitis Associated Protein family, and HIP-1 were identified as selectively up-regulated by H-1L-6. STAT-3 and SOCS-3 have been recognized in leptin signalling in vivo before. In this invention it is also demonstrated that leptin modulates the in vivo expression of the MT-II, Fnk and Pancreatitis Associated Protein I genes.
WO2007044318A3 Anti-hypercholesterolemic compounds This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.
WO2008039420A3 Novel inhibitors of beta-lactamase A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are β-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds are suitable for use with β-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
EP1758888B1 Butyrylcholinesterase selective inhibitors The invention provides butyrylcholinesterase inhibitors of formula (I), which contain an heterocyclic moiety and a 4 piperidine moiety with a linker in between. The compounds show a very high activity and selectivity towards BuChE, making them useful for the treatment and/or prophylaxis of cognitive disorders and/or neurodegenerative disorders.
WO2011009039A2 Pharmaceutical for oral delivery comprising mgbg and methods of treating disease Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.
WO2013091539A1 Pyrrole six-membered heteroaryl ring derivative, preparation method therefor, and medicinal uses thereof The present invention relates to a pyrrole six-membered heteroaryl ring derivative, the preparation method therefor, and the medicinal uses thereof. Specifically, the present invention relates to a new pyrrole six-membered heteroaryl ring derivative as represented in formula (I), the preparation method therefor, a medicinal composition comprising the derivative, and a therapeutic agent using same, and, in particular, the uses as a JAK inhibitor and an immunosuppressor. Substituents in formula (I) have the same definitions as in description.
CN101687810A Bicyclic compound and pharmaceutical use thereof Disclosed is a compound represented by the following formula: (wherein R<1> presents an optionally substituted hydrocarbon group, an optionally substituted amino group, an optionally substituted hydroxy group or an optionally substituted heterocyclic group; R<2> represents a hydrogen atom or an optionally substituted hydrocarbon group; Xa and Xb each represents C, N, O or S; Xc and Xd each represents C or N; m represents a number of 0-2; n represents a number of 1-3; ring A represents an optionally substituted 5-membered ring; ring B represents an optionally substituted 6-membered ring; and ring C represents an optionally substituted 3- to 5-membered ring; provided that when Xa, Xc and Xd are C, Xb is N or S) or a salt thereof, which is useful as an agent for prevention/treatment of diseases associated with action of melatonin.
US20110237628 Cyclopentyl- and cycloheptylpyrazoles This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula I wherein A and R1 to R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. The invention relates also to compositions including these compounds and methods of using the compounds.
CN101856349A Curcumenol medicament for treating cancer and production method The invention discloses a curcumenol medicament for treating cancer and production method. In the invention, the curcumenol, which is extracted from zedoary turmeric oil and purified, is dissolved in an oil solvent of black currant oil or borage oil. The curcumenol medicament comprises 0.1 to 25 weight percent of curcumenol, 20 to 99.9 weight percent of black currant oil or borage oil, and 0 to 30 percent of auxiliary material. The curcumenol can be dissolved in the oil solvent of black currant oil or borage oil when crystallization does not start or just starts after the curcumenol is purified. The curcumenol is not crystallized any longer, so the medicament can give full play to effect. The crystallized curcumenol is delivered into a high-speed cutting machine to be ground till the particle size is less than 0.1 mu m; and the ground curcumenol is dissolved in the oil solvent and can be made into various tablets, hard capsules, soft capsules, particles, oral liquid and other oral preparations.
CN103405451A Application of Chukrasone A in medicaments for treating tongue carcinoma The invention discloses an application of Chukrasone A in preparing medicaments for treating tongue carcinoma, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluations finds that the Chukrasone A also has a significant inhibitory effect on the growth of human tongue carcinoma cell strains Tca8113 and T6. Therefore, the Chukrasone A can be used for preparing anti-tongue carcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating tongue carcinoma provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to tongue carcinoma cells.
CN101748125A siRNA segment and application thereof used for curing and/or preventing Porcine Reproductive and Respiratory Syndrome The invention provides a siRNA segment and application thereof used for curing and/or preventing Porcine Reproductive and Respiratory Syndrome. Both the siRNA segment and a carrier comprising the siRNA segment play the protection role on the Marc145 clones inflected by PRRSV; the siRNA segment is discovered to be capable of reducing the mRNA level of PRRSV-M protein by about 30 percent-50 percent through real-time quantitative PCR and immunoblot assay; therefore, the siRNA segment and the carrier comprising the siRNA segment of the invention can be used for preparing drugs used for curing and/or preventing Porcine Reproductive and Respiratory Syndrome, and have important values on curing Porcine Reproductive and Respiratory Syndrome with genes.
US20100286128 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives useful as nicotinic acetylcholine-receptor ligands This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
CN103585134A Composition of fenofibric acid slow-release capsule and preparation method of same The invention discloses a composition of a fenofibric acid slow-release capsule, and a preparation method of the composition. The composition is prepared by mixing fenofibric acid, sodium alginate and calcium chloride. The fenofibric acid slow-release capsule prepared by using the preparation method is simple in prescription, simple in process and controllable in quality.
WO2010122571A3 A process for the selective methylation of erythromycin a derivatives. A process for selective methylation at 6 position of erythromycin A derivatives.
US20100227867 Compounds, Formulations, and Methods for Treating or Preventing Inflammatory Skin Disorders In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below: wherein each of R1, R2, and R3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R4 and R5 is independently hydrogen, alkyl, or alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A1, A3, and A4 is independently hydrogen or alkyl; and A2 is independently hydrogen or hydroxy; and wherein each of B1, B2, and B3 is independently hydrogen, hydroxy, or alkoxy; and each of B4 and B5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat inflammatory skin disorders and the symptoms associated therewith.
US7189741 Indolylpiperidine derivatives as antihistaminic and antiallergic agents The invention relates to indolyl piperidinyl derivatives of formula (I) wherein: A1 represents an alkylene, alkyleneoxy, alkylenethio, alkanoylene or hydroxyalkylene group; A2 represents an alkylene, alkyleneoxy, alkylenethio, alkanoylene or an alkyleneoxyalkylene group; W1 represents a phenylene, furanylene or pyridinylene group which is unsubstituted or substituted by one or more halogen atoms, alkoxy groups and/or alkyl groups; W2 represents a 3–10 membered monocyclic or bicyclic group containing from 1 to 3 heteroatoms said group being unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups and/or oxo groups; R1 represents a hydrogen or halogen atom or an alkyl, alkoxy or methylamino group; and R2 represents a carboxyl group; and pharmaceutically acceptable salts thereof; to processes for their preparation; to pharmaceutical compositions containing them; and to their medical use as antihistaminic and antiallergic agents.
CN101947314A Novel aqua for treating beriberi and preparation process thereof The invention relates to a novel aqua for treating beriberi and a preparation process thereof. The novel aqua for treating the beriberi comprises the following materials in part by mass: 0.1 to 0.3 part of trivalent silver ion compound, 0.2 to 0.4 part of keratinase, 0.5 to 5 parts of water soluble keratin and 100 parts of water. The preparation process comprises the following steps of: respectively weighing 0.1 to 0.3 part of trivalent silver ion compound, 0.2 to 0.4 part of keratinase, 0.5 to 5 parts of water soluble keratin and 100 parts of the water, and then completely stirring and uniformly mixing the materials until the mixtures is transparent. Clinical application shows that the novel aqua for treating the beriberi has the following effects and characteristics of: diminishing inflammation, relieving pain and killing bacteria because the selected trivalent silver ion compound has strong capability of killing fungus, bacteria and the like, dissolving necrotic keratin because the selected keratinase has a good function of dissolving necrotic stratum corneum so as to smoothen skin, and repairing skin because the selected water soluble keratinase can promote the cell growth and the collagen synthesis, repair the fungus degraded damaged corneum and cortex and smoothen skin.
EP1993579A2 A pharmaceutical composition for the prevention/treatment of bone disorders and a process for the preparation thereof Osteoporosis is one of the major problems in our aging society. Osteoporosis results in bone fracture in older members of the population, especially in post-menopausal women. In traditional medicine, there are many natural crude drugs that have the potential for use to treat bone diseases. So far, there is no report in literature on anti- osteoporosis (bone forming) activity of Butea species. It was thought to study the anti- osteoporotic activity of this plant. Thus, the present invention provides a pharmaceutical composition from the extracts of Butea monosperma for prevention or treatment of bone disorders, process of preparation and use thereof.
EP2270191A1 Preparation of microbial oil containing polyunsaturated fatty acids The present invention provides a process for the production of a microbial oil comprising culturing a micro-organism in a two stage fermentation process where, in a last stage that precedes the end of fermentation, the carbon source is: consumed by the micro-organisms at a rate greater than it is added to the medium; added at a rate ≤ 0.30 M carbon/kg medium; or is rate limiting on the growth of the micro-organism. The micro-organisms thus have the carbon source restricted so that they preferentially metabolise fats or lipids other than arachidonic acid (ARA), so increasing the proportion of ARA in the cells. A microbial oil is then recovered from the micro-organism, using hexane as a solvent, that has at least 50% ARA and at least 90% triglycerides.
EP2155674A1 Aminoalkoxy aryl sulfonamide compounds and their use as 5-ht6 ligands The present invention relates to novel aminoalkoxy arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardiovascular diseases and cancer.
CN101485751B Cotinus coggygria compound preparation and use The invention relates to a cotinus coggygria scop compound preparation, which is prepared from cotinus coggygria scop, rhizoma corydalis and hawkthorn in proportion, wherein the dosage of the cotinus coggygria scop is equal to that of the hawkthorn, and the dosage of the rhizoma corydalis is not more than 2/3 of that of the cotinus coggygria scop or the hawkthorn. The cotinus coggygria scop compound preparation can be used as an anticoagulant and antithrombotic drug, an abirritation drug, a drug for activating blood circulation to dissipate blood stasis and reducing the whole blood viscosity,a drug for improving the organism anti-hypoxia effect, and a drug for treating coronary heart disease or coronarism or miocardial infarction. The cotinus coggygria scop compound preparation not only improves the curative effect of the cotinus coggygria scop, but also reduces the dosage, and is used for easing pain and treating cardiovascular and cerebrovascular disease. Comparative experiments prove that the compound preparation has equivalent anticoagulant activity and abirritation as aspirin, and has the function of organism hypoxia resistance.
US20110136849 Process for reducing contaminating michael acceptor levels in oxycodone and other compositions The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
US20120058085 Deuterium Modified Benzimidazoles This invention relates to derivatives of 1-(p-chlorobenzyl)-2-(1-pyrrolidinylmethyl)benzimidazole according to Formula I wherein at least one Y is deuterium described herein and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of hepatitis C virus (HCV) RNA replication.
WO2012089465A3 Use of 13-hydroxy-9,11-octadecadienoic acid for tanning human skin, for dyeing human hair and for treating polymorphous light dermatosis The invention relates to the use of 13-hydroxy-9,11-octadecadienoic acid for tanning human skin and of methods associated therewith.
US20070203185 Therapeutical Composition Containing Dentritic Cells And Use Thereof The present invention relates to a method for the preparation of a therapeutical composition, in particular, the present invention relates to a method for treating dendritic cells with a combination of at least one interferon gamma receptor agonist and at least one toll like receptor 2 and/or TLR 6 agonist and using these pretreated dendritic cells for the preparation of a therapeutical composition. Moreover, the present invention relates to a therapeutical composition containing dendritic cells and the use thereof for the treatment of various diseases and disorders.
CN102936254A Drug composition containing ceftizoxime sodium compound The invention relates to the field of medicine and particularly relates to a ceftizoxime sodium compound which is a crystal. The ceftizoxime sodium crystal is determined through X-ray powder diffraction, and characteristic peaks of the ceftizoxime sodium crystal are displayed at the position of 2 theta which includes 9.6 degrees, 11.7 degrees, 13.5 degrees, 14.7degrees, 15.2 degrees, 15.7 degrees, 16.3 degrees, 19.4 degrees, 22.5 degrees, 25.4 degrees, 27.2 degrees and 33.2 degrees. The ceftizoxime sodium compound is not prone to absorb moisture and is good in liquidity. The invention further provides a preparation method of the ceftizoxime sodium compound and a drug composition containing the ceftizoxime sodium compound.
CN1623554A Anticancer auxiliary medicine using C-K as effective component and its application An auxiliary anticancer medicine for increasing the curative effect of other anticancer medicines, decreasing their toxin, preventing and treating the leukocytopenia and tissue injury caused by radiotherapy and chemicotheraphy, and improving immunity is prepared from ginsenoside C-K and the pharmacologically acceptable carrier or assistant.
EP1165071B1 Improved cancer treatment with temozolomide A method for treating a patient afflicted with cancer is provided, in which temozolomide is administered to the patient for at least two cycles of a cyclical dosing schedule, wherein each cycle has a dosing period of 5 to 25 days, in which temozolomide is administered daily, at a dose of 40 to 150 mg/m<2>/day, followed by a rest period of 5 to 14 days in which temozolomide is not administered. Also provided is a medical kit for administering temozolomide, having printed instructions for administering temozolomide according to the cyclical dosing schedule set forth above, and a supply of temozolomide in dosage units for at least one cycle, wherein each dosage unit contains 5 to 250 mg of temozolomide and a pharmaceutically acceptable carrier.
CN101057830A Naloxone hydrochloride sublingual spraying drug delivery system or composition and its preparation method The invention discloses a chlorhydric acid naloxone hypoglossal spraying drug delivery system or compound and the preparing method, belonging to pharmacology field. It is characterized in that: it is hypoglossal spraying agent, and the comprised components and their weight proportion are as follows: (1) chlorhydric acid naloxone or naloxone free alkali or naloxone medical salt: 0. 1-30%, (2) absorption promoter: 0. 5-10%; (3) osmotic pressure regulator: 0. 1 -5%; (4) bodying agent: 0. 5-30%; (5) corrigent: 0. 01-20%; (6) conservative 0. 01-0. 5%, (7) water: 45-95%. The invention is characterized by good adjustment, especially suitable for patient in comatose state; high biological utilization rate, convenient utilization. The product is characterized by stable performance, controllable quality and no stimulation to mouth mucosa.
CN102512447A Preparation for treating local ichthyosis and hand palm and foot sole keratinization The invention discloses a preparation for treating local ichthyosis and hand palm and foot sole keratinization. The preparation consists of the following components in percentage by mass: 5-15 percent of white oil, 1-8 percent of white vaseline, 1-3 percent of monoglyceride, 2-6 percent of octadecanol, 0.5-2 percent of span 60, 0.1-0.5 percent of methylparaben, 0.1-0.3 percent of propylparaben, 1-3 percent of vitamin E, 3-6 percent of glycerol, 1-3 percent of tween 60, 25-35 percent of urea, 0.01-0.1 percent of vitamin A acid and 35-40 percent of pure water. The invention develops an ointment with a stronger cutin softening effect aiming at the conditions of local ichthyosis and hand palm and foot sole keratinization; and the use method is that the preparation can be smeared at any time; and the preparation has no side effect.
CA2315953C 3'-epimeric k-252a derivatives Compounds defined by general structure (II) are disclosed. These compounds display pharmacological activities, including inhibition of tyrosine kinase activity and enhancement of the function and/or survival of trophic factor responsive cells, e.g., cholinergic neurons.
EP2398786A1 4 -isopropylphenyl glucitol compounds as sglt1 inhibitors The present invention provides 4-isopropylphenyl glucitol compounds which have no tendency to accumulate in the body and which inhibit SGLT1 activity to suppress postprandial hyperglycemia (or impaired glucose tolerance) through suppression of glucose absorption in the small intestine, whereby the compounds, for example, can suppress the onset of diabetes and metabolic syndrome or can treat these diseases. A 4-isopropylphenyl glucitol compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: [Chem. 1] wherein R1 represents a hydrogen atom, etc., R2 represents a methyl group, etc., R3 represents a C1-4 alkyl group substituted with an amino group(s), etc., and R4 represents a hydrogen atom, etc.
WO2009043307A1 Medicine composition containing abafungin The medicine composition containing abafungin is provided in the present invention, and the said composition contains abafungin and other antibacterial agents. The use of the said medicine composition for treating fungus infections or fungus and bacteria mixed infections is also provided in the present invention.
US20120093761 Vaccine compositions and methods of use thereof Nanoparticle-based vaccines, compositions, kits and methods are used for the effective delivery of one or more antigens in vivo for vaccination and antibody (e.g., monoclonal antibody) production, and for the effective delivery of peptides, proteins, siRNA, RNA or DNA to PAPCs or MHC class II positive cells (e.g. tumor cells). Antigens may be, for example, DNA that results in expression of the gene of interest and induction of a robust and specific immune response to the expressed protein in a subject (e.g., mammal). Antigens may also be immunogenic peptides or polypeptides that are processed and presented. In one embodiment, a nanoparticle -based method to deliver antigens in vivo as described herein includes injection of a vaccine composed of a DNA encoding at least one antigen, or at least one antigenic peptide or polypeptide conjugated to a charged dendrimer (e.g., PADRE-derivatized dendrimer) that is also conjugated to a T helper epitope (e.g., PADRE). Negatively-charged plasmids bind naturally to a positively-charged PADRE-dendrimer, while peptide or polypeptide antigens can be chemically linked to the PADRE-dendrimer if they are not negatively-charged. Alternatively, negatively-charged dendrimers may be used. The compositions, kits, vaccines and methods described herein have both prophylactic and treatment applications, i.e., can be used as a prophylactic to prevent onset of a disease or condition in a subject, as well as to treat a subject having a disease or condition. A vaccine as described herein can be used to mount an immune response against any infectious pathogen or cancer.
CN101828661A Health-care food for improving moisture of skin and removing wrinkle The invention discloses a health-care food for improving the moisture of skin and removing wrinkles, which is prepared by the following raw materials in parts by weight; 10-15 parts of collagen powder, 6-8 parts of soybean isoflavone, 3-5 parts of pearl powder, 3-5 parts of aloe extract, 3-5 parts of American ginseng extract, 3-5 parts of poria cocos extract, 3-5 parts of amur corktree bark extract, 2-3 parts of Chinese date, 1-2 parts of vitamin C powder, 3-5 parts of fructo-oligosaccharide, 3-8 parts of sodium carboxymethylcellulose, 1-5 parts of citric acid, 1-5 parts of malic acid and 5-20 parts of sucralose. The invention has the functions of internally expelling the toxin, tonifying the qi and nourishing the yin and replenishing the collagen lacked in human bodies by reasonably blending with the collagen powder, the soybean isoflavone, the pearl powder, the aloe extract, the poria cocos extract, the American ginseng extract, the amur corktree bark extract, the Chinese date and the vitamin C powder, thereby achieving the effects of water replenishing and wrinkle removal from inside to outside; and in addition, the raw materials of the fructo-oligosaccharide and the like are added, thereby the invention has the effects of adjusting tastes and promoting intestinal absorption.
US20080233121 Therapeutic treatments based on administration of small RNA fragments This invention provides therapeutic treatments that prevent or ameliorate thrombocytopenia based on administration of small RNA fragments. More specifically, this invention provides an improved chemotherapeutic regimen that prevents or ameliorates bone marrow suppression and thrombocytopenia induced by anti-cancer drugs, wherein the chemotherapeutic regimen incorporates administration of small RNA fragments. Further, the present invention provides a therapeutic treatment for thrombocytopenia associated with immune disorders known as Immune Thrombocytopenic Purpura based on administration of small RNA fragments.
WO2011037467A1 Atazanavir for treating inflammatory diseases The invention relates to Atazanavir for use as a medicament for preventing, treating and/or delaying an inflammation-mediated or -associated disease and/or a disease wherein oxidative stress occurs.
EP1023315B1 Methods and compositions for destruction of selected proteins Compounds having an ansamycin antibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic leading to the degradation of proteins and death of the targeted cells. These compositions may have different specificity than the ansamycin alone, allowing for a more specific targeting of the therapy, and can be effective in instances where the ansamycin alone has no effect. Thus, these compounds provide an entirely new class of targeted chemotherapy agents with application, depending on the nature of the targeting moiety, to treatment of a variety of different forms of cancer. Such agents can further be used to promote selective degradation of proteins associated with the pathogenesis of other diseases, including antigens associated with autoimmune disorders and pathogenic proteins associated with Alzheimer's disease. Exemplary targeting moieties which may be employed in compounds of the invention include testosterone, estradiol, tamoxifen and wortmannin.
CN101885748A Puerarin-7-O-glucuronide as well as preparation method and application thereof The invention relates to puerarin-7-O-glucuronide as well as a preparation method and application thereof. The molecular formula of the puerarin-7-O-glucuronide is C27H28O15, and the molecular weight is 592.14. The preparation method of the puerarin-7-O-glucuronide is characterized by comprising the steps of collecting rat urine, spirally steaming and concentrating in a water bath and separating and purifying to obtain the puerarin-7-O-glucuronide. The puerarin-7-O-glucuronide has the activity of scavenging 2,2-biphenylyl-1-picrylhydrazyl radicals and hydroxyl radicals. The puerarin-7-O-glucuronide has better antioxidation, solves the problems of poor puerarin dissolubility and low oral bioavailability and can provide a novel medicament for preventing and curing cardiovascular and cerebrovascular diseases, the preparation method is simple and is easy to implement without needing complicated process, and the puerarin-7-O-glucuronide has low cost and high purity, can be used as a standard substance for puerarin metabolic research and has radical scavenging activity.
CN101195646A Production method of stilbene glycoside extract The invention discloses a preparation method of stilbene glucoside, which comprises (1), adding polygonum multiflorum thumb with alcohol, heating and refluxing, filtering extract, recovering alcohol in the extract, concentrating until no alcohol smell left, obtaining concentrated solution or extract, (2), adding water into the concentrated solution or extract, mixing uniformly, standing, filtering and extracting the filtrate via acetic ester, (3), recovering acetic ester of extract liquid, concentrating to condensed ointment, drying and breaking to obtain stilbene glucoside. The inventive extract has stilbene glucoside content higher than 55%, with high yield, high product quality and simple process or the like.
WO2013007986A1 Orvinol and thevinol derivatives useful in the treatment of drug and alcohol abuse The invention provides orvinol and thevinol compounds useful for the treatment of drug and alcohol abuse, the compounds being particularly useful for the prevention of relapse in recovering addicts.
EP1720880A1 C8, c8' linked 5-oxo-1,2,3,11a-tetrahydro-5h-pyrrolo[2,1-c][1,4]benzodiazepine dimers with 1h-pyrrole-dicarboxylic acid amide linkers and oligomeric analogs thereof as well as related compounds for the treatment of proliferative diseases Compounds of formula (I): PBD-A-Y-X- (Het)na-L- (Het)nb-L- (Het)nc-T- (Het')nd-L- (Het')ne-L- (Het')nf-X' -Y' -A' -PBD' and salts, solvates and chemically protected forms thereof, are disclosed wherein the PBD units have the formulae (PBD) (PBD') with the bonds at the 8 position on each molecule bond to the A and A' groups respectively ; A is selected from O, S, NH or a single bond , and each Het and Het' is respectively an amino-heteroarylene-carbonyl group ; X and X' are both either NH or C (=O) -Q-C (=O) - wherein Q is a divalent group such that HY = R ; in a second aspectm the invention comprises compounds of the general formula (II) : PBD-A-Y-X-(Het)ng-[L-(Het)nh] nj-X' -Y' -A' -PBD'. Wherein : PBD and PBD' are as defined above, X and X' are either NH and C(=O) respectively or C(O) and NH respectively ; the other substituents are defined in the claims. Further aspects of the present invention relate to their use in the manufacture of a medicament for the treatment of a proliferative disease.
CN101690714A Antimicrobial, antiprotozoal and antitumor allicin liposome and preparation method thereof The invention relates to an allicin composition and a preparation method of a preparation thereof. The antimicrobial, antiprotozoal and antitumor allicin liposome is characterized by comprising 1 to 6.5ml of allicin, 10 to 50ml of cosolvent and 100ml of medicinal soybean oil, wherein the cosolvent is one of tween-80, tween-100 or lecithin. The preparation method comprises the following steps: 1, according to the proportion, slowly pouring the cosolvent in a container containing allicin and stirring continuously; 2, keeping stirring and adding the soybean oil till the total dose reaches 100ml; and 3, subpackaging the mixture into 300 soft capsules or gelatin pills. The allicin composition has the characteristics of hydrophilicity and lipophilicity, thereby extending the application of allicin from bacterium resistance and fungus resistance to virus resistance, protozoan resistance and tumor resistance; and the composition is expected to solve problems which western medicine cannot overcome.
WO2008051808A2 Bicyclic triazoles as protein kinase modulators The present disclosure provides bicyclic triazole protein kinase modulators of formula I: and methods of using these compounds to treat diseases mediated by kinase activity.
CN101157710A Method for preparing iron supplementary carboxymethyl Chitosan oligosaccharide ferrous The invention relates to a preparation method of iron supplement agent-ferrous carboxymethyl chitooligosaccharide. The preparation method is as following: 100ml of 0.1 mol/l ferrous ammonium sulfate solution is prepared, the pH value is adjusted to 6, 4g of carboxymethyl chitooligosaccharide is added, anti-oxidation stabilizer is added, the mixture is stirred constantly, the reaction temperature is controlled at 25 DEG C and the reaction time is 1 hour. The sediments are filtrated and vacuum dried, the drying temperature is at 60 DEG C so as to prepare the ferrous carboxymethyl chitooligosaccharide, wherein, the content of ferrous is 0.46mmol/g. Wherein, the preparation of the anti-oxidation stabilizer is that the thiourea and the water solution of nickel acetate are mixed evenly to get the anti-oxidation stabilizer. The invention has the advantages that: the invention does not need the nitrogen for protection by adding the anti-oxidation stabilizer; furthermore, compared with the technical routes with the nitrogen protection, the yield can be increased appropriately, then the requirements of the conditions and the equipments for the reaction are much milder, which is beneficial to the industrialization. The ferrous carboxymethyl chitooligosaccharide is a natural modified product, of which the safety and the bioactivity are better than other iron supplement agents.
US20090221610 Compositions and Methods for Treating Cognitive Disorders The present invention relates to the use of inhibitors or blockers of Ih (hyperpolarization-activated cationic current) channels in the treatment of cognitive disorders. In preferred aspects of the present invention, an effective amount of a compound is administered to a patient in need, wherein the compound has the chemical structure: Where R1 is H, or an optionally substituted C1-C3 alkyl, preferably a C2 alkyl (ethyl) group; R2 is an optionally substituted C1-C3 alkyl group, preferably a methyl group; R3 is H, an optionally substituted C1-C3 alkyl (preferably methyl), a halogen or 0(Ci-Ca) alkyl; R4 is an optionally substituted C1-C6 alkyl, C(O)—(C1-C5)alkyl, C(O)-aryl, C(O)O—(C1-C4)alkyl, C(O)O-aryl, or an optionally substituted heterocyclic, aryl or heteroaryl group; R4 is H or an optionally substituted C1-C6 (preferably a C1-C3) alkyl; R5, R6 and R7 are each independently H, halogen, an optionally substituted C1-C6 alkyl (preferably, an optionally substituted C1-C3 alkyl), 0-(C1-C3) alkyl, or an optionally substituted heterocyclic, aryl or heteroaryl group; Y− is an anion of a pharmaceutically acceptable salt (a physiologically acceptable anion, preferably a Cl−, Br−, I−, OAc−); or a solvate or polymorph thereof, optionally, in combination with guanfacine and/or chelerythrine, and a pharmaceutically acceptable carrier, additive or excipient to a patient in need of therapy.
EP1675835B1 Methods of preparation of dehydro-diketopiperazines in liquid phase or on solid supported phase The preparation of any compound of the generic structure (I); wherein: R1 and R2 are substituents described in the main text. Cycl- is a group represented by either of the formulae (a) and (b); wherein: R3 to R8, X and Y are substituents described in the main text. The above described compounds may be used for the treatment of cancer. The preparation method consists of coupling of the amine group of phosphynilglycinate with the carboxylic group of an aminoacid, the successively coupling of the above formed compound with the formyl-Cycl derivative, the deprotection of the aminoacid and the formation of dehydro-diketopiperazine employing mild alkaline conditions. The method is extended for the preparation of individual derivatives or libraries of derivatives related to the above described compounds of the general formula (II), employing a solid supported phosphonate of the general formula (II), wherein: Res represents any polymer support (resin) with or without a linker, Prot represents any NH- protective group, R represents alkyl or alkyloxyalkyl groups.
EP1370558B1 Piperazine- and piperidine-derivatives as melanocortin receptor agonists The present invention relates to melanocortin receptor agonists of formula I,which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction.
US20100196447 Silk biomaterials and methods of use thereof The present invention provides an all-aqueous process and composition for production of silk biomaterials, e.g., fibers, films, foams and mats. In the process, at least one biocompatible polymer, such as poly(ethylene oxide) (PEO) (a well-documented biocompatible material), was blended with the silk protein prior to processing e.g., electrospinning. We discovered that this step avoids problems associated with conformational transitions of fibroin during solubilization and reprocessing from aqueous solution which lead to embrittled materials. Moreover, the process avoids the use of organic solvents that can pose problems when the processed biomaterials are exposed to cells in vitro or in vivo.
CN103200934A Pharmaceutical composition for treating HCV infections The present invention relates to a granular pharmaceutical composition comprising an HCV protease inhibitor and at least one poloxamer.
US20110172257 (poly) aminoalkylaminoalkylamide, alkyl-urea, or alkyl-sulfonamide derivatives of epipodophyllotoxin, a process for preparing them, and application thereof in therapy as anticancer agents The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: —R represents hydrogen or C1-4alkyl, —A represents CO(CH2)n or CONH(CH2)n where n=2, 3, 4, or 5, —R1 and R2 are as described herein.
CA2446254C New synergetic compositions of vitamins, minerals and trace-elements to stimulate the elimination of intra-cellular lipid deposits Nearly 40% population of the developed countries in the world have the problem of excess weight. Up till now, no correlation was established between the deficiencies of certain specific vitamins , minerals and trace-elements with the problem of excess weight. None of the weight reduction strategies proposed till today took into consideration the reduced capacity of the cells to eliminate the intracellular lipid deposits which is the real cause of excess weight. After many years of research, we discovered that a synergetic composition of certain specific vitamins, minerals and trace-elements stimulate the intracellular lipid elimination capacity of cells thereby helping to reduce body weight in a very short period of time without any side-effects and without the rebound effect often observed at the end of the dieting period. The methods of preparation of such solid or liquid compositions for oral or topical application are known. These synergetic compositions can be used either alone or in association with products commonly used to reduce weight, with specific diets, with apparatuses for physical exercise or muscular electrostimulation which are commonly employed to increase energy loss.
US20110256249 Hair and scalp care formulations for treating and preventing acne and related skin conditions The present invention is directed to skin treatment formulations having salicylic acid and other secondary ingredients. The secondary ingredients may include: non-comedogenic essential oils and plant extracts and sebum reducing agents. Salicylic acid and the secondary ingredients are provided in amounts effective to provide a sufficiently aggressive skin treatment for unclogging pores and reducing inflammation, while maintaining levels of sebum on the exterior of the skin to form an operative water barrier on the skin and hair. Additionally, a method is provided that unclogs pores, reduces inflammation, and controls levels of sebum on the exterior of the skin to maintain an operative water barrier on the skin and hair. The method may include, applying a sufficiently aggressive product comprising salicylic acid, non-comedogenic plant extracts and essential oils, and a sebum reducing agent to hair and its surrounding areas.
WO2009080722A2 Carboxylic derivatives for use in the treatment of cancer The invention provides novel compounds of formula (I), wherein: R1 is a radical derived from one of the known ring systems; R2 is a phenyl radical optionally substituted; Xn represents a birradical selected from the group consisting of: -(CH2)1-4-, (C2-C4)-alkenyl, (C2-C4)alkynyl, -S-(CH2)1-3-#, and - (CH2)1-3-O-#; wherein the symbol # indicates the position at which Xn is attached to R1; Yn is a birradical selected from the group consisting of: - (CH2)2-4-, -S-(CH2)1-3#, and -O-(CH2)1-3-#,; wherein the symbol # indicates the position at which Yn is attached to R2; and R3 is a radical selected from the group consisting of: -OR4. The compounds of formula (I) are useful in the treatment of cancer.
US7589219 2,5-bis-diamine-[1,4]benzoquinonic derivatives, useful for the treatment of alzheimer's disease, method for preparing them and intermediates of said method 2,5-bis-diamine-[1,4]benzoquinonic derivatives, having a general formula (I) have proved useful for the treatment of Alzheimer's disease; a method for preparing them and intermediates used in said method are also described.
US20120117672 Isolation and growth of stem cells from hemangiomas The present invention describes stem cells and progenitor cells derived from hemangiomas, including testing of angiogenic inhibitors using these cells. The invention as described is useful in providing a process to culture and propagate hemangioma stem cells and generate xenograft models to develop treatments for infantile hemangiomas and other types of vascular lesions.
US20100087441 Prognostic Method A method for prognosing a rheumatoid arthritis phenotype using the outcomes of selected single nucleotide polymorphisms (SNPs) and clinical variables. A method for genotyping multiple rheumatoid arthritis associated genetic variations comprising use of a DNA microrarray. A microarray for use in the described methods.
CA2306830C Use of adamantane amines or structurally similar compounds for combating borna disease virus and for the prevention and treatment of affective diseases and other disorders associated with bdv infections in humans and animals The invention concerns the use of 1-adamantane amines (amantadines) or structurally similar compounds for combating boma disease virus infections and for treating affective diseases and disorders associated with borna disease virus infections in humans and animals. The use of these substances results in rapid and lasting elimination of the symptoms and signs and in the suppression of the virus activity.
WO2009024516A1 Novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives useful as nicotinic acetylcholine receptor ligands This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as thoserelated to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
WO2006013049A2 Benzyloxy derivatives as maob inhibitors The present invention relates to compounds of the general formula (I); wherein Rl is halogen; R2 is -C(O)NH2,-C(NH2)=N-OH, -C(O)CH2Br, -C(O)N(CH3)OCH3 or-C(O)-lower alkyl, or is a 5-membered heteroaryl group, containing 2 or 3 heteroatoms, selected from the group consisting of N, O or S, optionally substituted by R3, wherein R3 is lower alkyl, -NR'R' or -C(O)R; R is NR'R', lower alkyl, or lower alkoxy; R'/R' are independently hydrogen or lower alkyl; as well as their pharmaceutically acceptable salts for the treatment of diseases, which are mediated by monoamine oxidase B inhibitors, for example Alzheimer's disease and senile dementia.
WO2011009059A3 Method of treating or preventing cancer Disclosed is a method for inhibiting Akt, activating AMPK, inhibiting mTOR, treating or preventing development of cancer, and/or preventing progression of premalignant lesions to cancer in an animal comprising administering to the animal an effective amount of a compound as described herein, for example, NSC 743411, whose formula is set forth below. The method involves the use of these compounds as single agents or in combination with conventional chemotherapy, biological therapy, or radiation therapy. The invention further provides novel compounds and pharmaceutical compositions for use in treating or preventing development of cancer or preventing the progression of premalignant lesions into cancer. Also disclosed is a method of inhibiting CSF1R.
WO2013032558A4 Products for anti-inflammation support This disclosure provides products, including pharmaceutical compositions and dietary supplements, which are useful for anti-inflammatory support.
US7157495 Hexahydrofuro[2,3-B]furan-3-YL-N-{3-[(1,3-benzodioxol-5-ylsulfonyl)(isobutyl)amino]-1-benzyl-2-hydroxypropyl}carbamate as retroviral protease inhibitor Compositions comprising bis-tetrahydrofuran benzodioxyolyl sulfonamide compounds that are surprisingly effective protease inhibitors and a second antiretroviral compound are disclosed. Methods of inhibiting retrovirus proteases, in particular multi-drug resistant retrovirus proteases, methods of treating or preventing infection or disease associated with retrovirus infection in a mammal, and methods of inhibiting viral replication are also disclosed.
CN103420906A Novel tyrosine protein kinase inhibitor The invention provides a novel and effective tyrosine protein kinase inhibitor, its isomer, pharmaceutically acceptable salts and chemical protection form, and pharmaceutical composition of the novel tyrosine protein kinase inhibitor and a pharmaceutical carrier or a diluent. The novel tyrosine protein kinase inhibitor can effectively treat protein kinase abnormity-caused diseases, and can effectively inhibit c-Met or c-Met mutant, and ALK or ALK fusion protein.
US20130022676 Pulsatile drug release In one aspect, the present invention is concerned with a treatment where it is desired that an active agent is designed to be released in a pulse at a time point some time after administration of the active agent. The present invention is particularly suited to administering an agent which may be released whilst a subject is sleeping. As well as treating certain conditions by a particular regime, the invention also provides novel formulations for a delayed, followed by a pulsed release of drug.
WO2014102889A1 Antitumor agent and method for producing same The present invention provides: a very highly effective antitumor agent which has an extremely high effect especially on various leukemia, lymphoma and solid cancers including refractory ATL; and a method for producing the antitumor agent. A compound represented by general formula (I) (excluding a compound represented by formula (D)). (In formula (I), R1 represents a phenyl group that is substituted by at least one group selected from among a hydroxyl group, a methoxy group, a methylenedioxy group and a phosphoric acid group; R2 represents one group selected from among a hydrogen atom, a hydroxyl group, a methoxy group, an acetyl group, an anilino group and groups represented by formulae (II); R3 represents one group selected from among a hydrogen atom, a hydroxyl group, a methoxy group and an acetyl group; and R4 represents one group selected from among a hydrogen atom, a hydroxyl group, a methoxy group and an acetyl group.)
WO2013001490A1 Novel anti-inflammatory dihydrochalcone derivatives and use thereof Disclosed are dihydrochaicone derivatives useful in the treatment of inflammatory and neuro-inflammatory diseases such as Alzheimer and Parkinson or conditions such as stroke. Both a and β carbons of the dihydrochaicone are hydroxylated. Also disclosed are methods of using such compounds in the treatment of inflammatory diseases in mammals and pharmaceutical compositions containing such compounds.
US6946463 1,2,5,10-tetrahydropyridazino[4,5-b]quinoline-1,10-diones and their use for the treatment of pain Compounds according to structural diagram (I) are disclosed, wherein R1, A, E and D are as defined in the specification. Also disclosed are pharmaceutical compositions comprising a pain-ameliorating effective amount of a compound in accord with structural diagram (I). The following is an examiner's statement of reasons for allowance: In view of applicants' amendments to the claims which limit “E” to phenyl or cycloalkyl groups the rejections of the previous action no longer pertain as they at best teach “E” as alkyl.
WO2013167959A1 Myrrh based composition for otological use The present invention relates to a pharmaceutical composition or a medical device or a food supplement comprising a myrrh extract, preferably a myrrh oil extract or a myrrh hydroglyceric extract, for otological use or for oral use or for topical use, preferably for treating pediatric patients. In particular, the present invention relates to a myrrh extract, preferably a myrrh oil extract or a myrrh hydroglyceric extract, for relieving and/or preventing irritative states of pharynx (nasopharynx, oropharynx, laryngopharynx and hypopharynx), throat (pharyngitis and tonsillitis) and/or ear (otitis), which might be caused by infections (treatment of oropharynx infections) or by colds and/or allergies.
WO2014071449A1 Neuroactive steroids and their use to facilitate neuroprotection The present disclosure teaches generally neuroprotection and in particular the use of non-hormonal neuroactive steroids to ameliorate inflammation of the central nervous system (CNS). More specifically, the present claims define methods of treating inflammation or ameliorating a neuroinflammatory -promoting condition in the CNS by administration of a steroid with certain properties formulated in a sulfobutyl ether beta-cyclodextrin composition. The steroid is neuroactive, devoid of hormonal endocrine activity and activates a pregnane X receptor. Examples of such steroids include alphaxalone, alphadolone, allopregnanolone, pregnanolone, ganaxolone, hydroxydione, minaxolone, Org20599, Org21465, CT1341 and compounds of Formula (I). Dependent claims further define the type of the neuroinflammatory -promoting conditions, the type of cyclodextrin, the molar ratio of neuroactive steroid to the cyclodextrin and the inclusion of other active agents or excipients in the composition and their nature.
CN101342166B Application of hydroxyl benzoate and analogue in preparing medicament for preventing and treating hepatitis B virus The invention relates to the applications of paraben and analogues thereof in preparing medicine used for preventing and curing viral infection, in particular to the application of the medicine used for curing the HBV, HPV and HSV viral diseases of human and animal. The viral diseases comprise hepatitis B, herpes simplex, condyloma acuminate, vaginitis, cervicitis and cervical erosion. The applications are as follows: the paraben, the paraben analog and the various auxiliary materials of pharmacy are made into different drugs or personal care products.
EP2033643A1 Compressed preparation [Object] The present invention provides an olmesartan medoxomil-containing drug product having an improved dissolution property. [Means for Solution] A production method for an olmesartan medoxomil-containing drug product characterized in that the method comprises a process of compressing a composition.
CN103301145A Medical application of astragaloside The invention relates to the field of medicines, and in particular relates to medical application of astragaloside. The astragaloside can be applied to the preparation of medicines or health products used for improving the memory of normal human.
US20120108584 2h or 3h-benzo[e]indazol-1-yl carbamate derivatives, the preparation and therapeutic use thereof Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.
US20120071552 Zinc-Monocysteine Complex and Method Of Using Zinc-Cysteine Complexes A method of providing zinc to a subject in need of treatment includes administering to the subject an effective amount of a zinc-cysteine complex. The zinc-cysteine complex is preferably a zinc-monocysteine complex. The complexes of zinc-cysteine of the present invention increase the activity of antioxidant enzymes catalase and glutathione peroxidase, and the antioxidant protein metallothionein. The complexes of zinc-cysteine of the present invention protect retinal pigment epithelial cells from increasing hydrogen peroxide concentrations.
WO2012137967A1 Calcium phosphate microcapsule Provided is a microcapsule having a core-shell structure, the core being an oily substance and the shell being configured from calcium phosphate.
WO2014004674A3 Combination treatment of abt-450 and ritonavir and e.g. abt-072 and/or abt-333|for use in treating hcv In one aspect, the present invention features HCV therapies comprising administering to a patient in need thereof an HCV protease inhibitor (like ABT-450 (compound 1) or danoprevir) and a cytochrome P450 monooxygenase inhibitor like ritonavir or cobicistat, wherein ritonavir is used as a pharmacokinetic booster to improve the pharmacokinetics of the HCV protease inhibitor. The HCV therapies do not require the testing of total cholesterol and triglyceride levels prior to and after the therapies.
CN103070853A Use of ethyl pyruvate in drug preparation The present invention belongs to the field of drug preparation, and relates to a new drug use of ethyl pyruvate. According to the present invention, exogenous ethyl pyruvate is adopted; a series of whole animal experiments are performed, wherein results show that with the ethyl pyruvate, blood-brain barrier damage after brain injury can be lessened, brain tissue injury can be reduced, sensorimotor dysfunction restoration after brain injury can be promoted, and space learning and memory ability restoration can be promoted. In addition, the experimental results show that the ethyl pyruvate can be adopted as a treatment drug for treatment of blood-brain barrier damage after brain injury, and promotion of neurological function restoration after brain injury.
CN1594332A Glycyrrhetic acid and phospholipid composites of glycyrrhetate and process for preparing same The invention provides a glycyrrhetic acid and phospholipid composites of glycyrrhetate and process for preparing same by forming phospholipid compound in suitable dissolvent from glycyrrhizinic acid and its salts with a definite quantity of lecithin, thus converting the physical and chemical property, and improving the bioavailability of the glycyrrhizic acid and its salts.
US20090004253 Composite device for the repair or regeneration of tissue The present invention is directed to composite devices comprising a tissue-engineering scaffold and an anionic polysaccharide/structural protein coating. The composite devices are useful for the reparation and regeneration of tissue, particularly in the treatment of chronic wounds.
US20100010013 Dihydropyrimidine compounds and their uses in manufacture of a medicament for treatment and prevention of viral diseases The present invention relates to compounds of the formula (I) or pharmaceutically acceptable salts or hydrates thereof. The present invention further relates to processes for the preparation of the compounds of formula (I) and optical isomers and to use of the compounds of formula (I), isomers, pharmaceutically acceptable salts or hydrates thereof as medicaments, in particular as medicaments for the treatment and prevention of Hepatitis B.
WO2011056174A1 Migraine headache relief composition The present invention relates to the formulation of aqueous herbal supplement compositions for providing relief to a user suffering from migraine headaches. According to at least one aspect of the present invention, an aqueous herbal supplement composition is provided that is formulated to alleviate a number of the symptoms associated with migraine headaches. The aqueous herbal supplement composition is formulated from natural ingredients including Ubiquinone, Feverfew extract, and a Magnesium salt. In at least one embodiment of the present invention, the formulation of the aqueous herbal supplement composition further includes St. John's Wort extracts, Butterbur Root extracts, and vitamin B2. The formulation can optionally include sugar or other sweeteners and natural flavorings.
CN103393647A Application of Sarcaboside B to preparation of medicament for treatment and prevention of renal insufficiency The invention discloses application of Sarcaboside B to medicaments for prevention and / or treatment of renal insufficiency and belongs to the technical field of novel application of medicaments. The application of Sarcaboside B to the preparation of medicaments for preventing and treating renal insufficiency involved in the invention is disclosed for the first time. As the Sarcaboside B has a novel skeleton type and unimaginably strong activity in inhibition of renal insufficiency, no other compound can give any enlightenment. The invention has outstanding substantive distinguishing features and makes substantial progress in prevention and treatment of renal insufficiency.
US20080045590 Use of substituted cyclopropane acid derivatives for producing drugs for use in the treatment of metabolic syndrome Disclosed is the use of certain substituted cyclopropane acid derivatives of Formula 1 as defined herein and of their physiologically tolerated salts for treating metabolic syndrome and related disorders.
CN103040739A Drug composition containing docetaxel compound The invention provides a drug composition containing a docetaxel compound. The drug composition comprises docetaxel, tween-80, polyoxyethylene castor oil, citric acid and enthanol. A preparation method comprises the following steps: adding polyoxyethylene castor oil, citric acid and enthanol into tween-80, mixing uniformly, adding docetaxel, dissolving, and mixing uniformly to form a homogeneous and clear liquid. According to the drug composition, as docetaxel, tween-80, polyoxyethylene castor oil, citric acid and enthanol are compounded, the problem of poor dissolvability of docetaxel is effectively solved; the drug composition is high in qualification rate and good in long term stability; and as docetaxel is not precipitated easily when an infusion solution is added, the drug safety is improved. In addition, as the use amount of tween-80 is reduced, the hemolysis risk caused by tween-80 can be reduced.
WO2007065869A1 Labelled docetaxel There are provided deuterated docetaxel derivatives, characterized in that the isotopes are present in the tert-butoxy group. More particularly, one or more of the hydrogen atoms of the tert-butoxy group of docetaxel is replaced with deuterium (2H). A process for their preparation, their use as internal standard in analytical methods for determining docetaxel and their use in the treatment of leukemia/lymphoma and solid tumors, are also provided.
US20120302535 Progesterone treatment for improving sleep quality Described herein are therapeutic methods using progesterone and progesterone analogs to improve sleep quality. The methods may be particularly useful to treat subject with perturbed sleep patterns, such as subjects who suffer from mid-sleep period awakenings.
EP1495117A2 Human deubiquitinating protease gene on chromosome 7 and its murine ortholog Human and murine analogs of DUBs, hematopoietic-specific, cytokine-inducible deubiquitinating proteases, clustered on chromosome 7 and their respective regulatory regions are identified. The nucleotide or proteins encoded thereby may be used in assays to identify inhibitors of hDUB7 or mDUB7. The invention also includes transducing peptides comprising an NLS or transducing sequence of hDUB7 or mDUB7 linked to a cargo molecule, and methods of delivering a biologically active protein, therapeutically effective compound, antisense nucleotide, or test compound to a cell wherein a transducing peptide is added exogenously to a cell.
WO2010071583A1 Pharmaceutical product comprising a p38 kinase inhibitor and a second active ingredient The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclopropyl-3-fluoro-4-methyl-5-[3-[[l-[2-[2- (methylamino)ethoxy]phenyl]cyclopropyl]amino]-2-oxo-l(2H)-pyrazinyl]- benzamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a β2 adrenoceptor agonist; a CCRl antagonist; a chemokine antagonist (not CCRl); a corticosteroid; a CRTh2 antagonist; a DPI antagonist; an Ηistone Deacetylase activator; an IKK2 kinase inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; a MABA compound; an MPO inhibitor; a muscarinic antagonist; a PDE4 inhibitor; a PPARγ agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
WO2012016690A1 Use of glyceryl trinitrate for treating hematomas Use of glyceryl trinitrate (GTN) for treating hematomas.
WO2012134188A2 Novel oxazolidinone derivative and medical composition containing same The present invention relates to a novel oxazolidinone derivative indicated as chemical formula 1 on the description, and in particular, to a novel oxazolidinone compound having a cyclic amidoxime or a cyclic amidrazone group. In the chemical formula 1, R and Q are identical to as defined in the detailed explanation. In addition, the present invention relates to an antibiotic medical compound having the novel oxazolidinone derivative of the chemical formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, and a pharmaceutically permitted salt thereof, as active ingredients. The novel oxazolidinone derivative of the present invention, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically permitted salt thereof, have a wide antibacterial spectrum for resistant bacteria, have low toxicity, and show strong antibacterial effect on gram positive and gram negative bacteria, and is thereby useful as an antibiotic.
US20090324570 Photostabilization of Retinoids with Alkoxycrylene Compounds The photostabilizing electronic excited state energy—particularly singlet state energy from retinoid compounds—has been found to be readily transferred to (accepted by) α-cyanodiphenylacrylate compounds having an alkoxy radical in the four (para) position (hereinafter “alkoxycrylenes”) on one of the phenyl rings having the formula (I): wherein one of R1 and R2 is a straight or branched chain C1-C30 alkoxy radical, preferably C1-C8, more preferably methoxy, and the non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C30 alkyl radical, preferably C2-C20. The alkoxycrylene compounds of formula (I) significantly increase the photostability of retinoid compounds in a composition by at least 3-fold and as much as 10-fold or greater. The ability of the alkoxycrylene compounds to stabilize the retinoid compound is concentration dependent, with the amount of retinoid photostabilization increasing with the concentration of the alkoxycrylene compound.
WO2007045867A1 3 -aminoindole compounds as crth2 receptor ligands Compounds of formula [I] are CRTH2 antagonists, useful in the treatment o conditions having an inflammatory component: in which: R1, R2, R3 and R4 are independently hydrogen, (C1-C6) alky!, (C1-C6) haloalkyl, halo, -S(O)nR10, -NR11SO2R10, -SO2N(R11)2, -N(R11)2, -NR11C(O)R10, -C(O)N(R11)2, -CO2R11, -C(O)R10, CN or a group OR12; wherein each R10 is independently (C1-C6) alkyl, (C1-C6) haloalkyl, cycloalkyl, aryl, or heteroaryl; R11 is independently hydrogen, (C1-C6)alkyl, (C1-C6) haloalkyl, cycloalkyl, aryl, or heteroaryl; R12 is hydrogen, (C1-C6) alkyl, (C1-C6) haloalkyl, cycloalkyl, or a group -SO2R10, wherein n is O 1 or 2; R5 and R6 are independently hydrogen, (C1-C6) alkyl or (C1-C6) haloalkyl, or R5 and R6 together with the atom to which they are attached form a cycloalkyl group; R7 is hydrogen, (C1-C6) alkyl, or (C1-C6) haloalkyl; R8 is aryl, heteroaryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused- heterocycloalkyl or aryl-fused-cycloalkyl; and R9 is hydrogen, (C1-C6) alkyl, (C1-C6) haloalkyl, or cycloalkyl.
WO2006114703A3 Method of administration of (1s,s2) -1- (4 -hydroxyphenyl) -2- (4-hydr0xy-4-phenylpiperidin-1-yl) -1- propano (traxoprodil) The present invention in one aspect is directed to a method for improving the bio-availability of (IS, 2S) -1- (4-hydroxyphenyl) -2- (4-hydroxy-4-phenylpiperidin-l-yl) -1-propanol traxoprodil or a pharmaceutically acceptable salt thereof in a human, the method comprising administering over a period of time of at least 24 hours (IS, 2S) -1- (4-hydroxyphenyl) -2- (4-hydroxy-4- phenylpiperidin-1-yl) -1-propanol or a pharmaceutically acceptable salt thereof to the human, wherein the period of time over which (IS, 2S) -1- (4-hydroxyphenyl) -2- (4-hydroxy-4-phenylpiperidin-l-yl) -1-propanol or a pharmaceutically acceptable salt thereof is administered is the sum of a first period of time and a second period of time, wherein the rate of administration over the first period of time is greater than the rate of administration over the second period of time, wherein the bio-availability is improved relative to administration at a constant rate that is equal to the rate of administration over the second period of time.
US20110294737 Terminally-differentiated anucleate platelet progeny generation Platelets are induced to proliferate, form extensions and produce daughter cells by various methods, including culturing platelets under thrombocytopenic conditions. Expansion of platelet cell numbers increases the storage life of platelets. Modulation of RT activity can be used to produce new daughter platelets. Therefore, the invention provides a new therapeutic use for RT inhibitors that can now be used for treatment of thrombocytopenia and related disorders. Likewise, application of soluble protein factor that may be secreted and/or released by platelets cultured under thrombocytopenic conditions may also be used as a therapeutic agent to increase platelet numbers.
WO2006085497A1 Tablet disintegrating in the oral cavity It is intended to provide a tablet, which quickly disintegrates in the oral cavity, has an appropriate hardness and is suitable for the production on the industrial scale, and a method of producing the same. Namely, a tablet disintegrating in the oral cavity which comprises a) an active ingredient, b) a sugar or a sugar alcohol, c) a partly gelatinized starch containing from 10 to 20% by weight of matters soluble in cold water, and d) a disintegrating agent. The tablet disintegrating in the oral cavity as described above can be produced by blending the disintegrating agent with a granular mixture consisting of the active ingredient a), the sugar or the sugar alcohol b) and the partly gelatinized starch containing from 10 to 20% by weight of matters soluble in cold water c) followed by compression molding.
US7737143 such as 6-(1H-Benzimidazol-1-yl)-N-benzylpyrazin-2-amine, used as antidiabetic, anticarcinogenic and antiarthritic agents or for treating autoimmune diseases A compound of general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating kinase-associated disease states using the compound of formula (I) is also described.
US20100209345 Fluorinated Ligands for Targeting Peripheral Benzodiazepine Receptors The invention provides fluorinated compounds of formula (I): The compounds may be used in diagnosis or treatment of a disorder in a mammal characterised by an abnormal density of peripheral benzodiazepine receptors.
CN102525915A Sustained release injection preparation and preparation method and application thereof The invention relates to a sustained release injection preparation and a preparation method and application of the preparation. Specifically, the invention relates to a sustained release injection preparation, which comprises a psychotropic medication and a nonaqueous carrier and can be released in a sustained manner within at least one week. The sustained release injection preparation of the invention has the advantages of better sustained release effect, longer effect, better stability, simple dosage form, no need of lyophilization, eaier preparation process, lower cost, and more convenience for use.
US20120088736 [4-(6-HALO-7-Substituted-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENYL]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREAS and Forms and Methods Related Thereto The present invention provides novel sulfonylurea compounds of formula (I) and pharmaceutically acceptable derivatives and polymorph and amorphous forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or forms thereof.
EP1614420A2 Treatment of hypertension, angina and other disorders using (-) amlodipine Methods and compositions are disclosed utilizing the optically pure (-) isomer of amlodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liabiliy of adverse effects associated with the racemic mixture of amlodipine. The (-) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of (-) amlodopine as a calcium channel antagonist such as cerebral ischemia, cerebral disorders, arrhythmias, cardiac hypertrophy, coronary vasospasm, myocardial infarction, renal impairment and acute renal failure, without the concomitant liability of adverse effects associated with the racemic mixture of amlodopine.
WO2008024893A3 Derivatives of uric and thiouric acid for oxidative stress-related diseases Disclosed is a method of treating or preventing an oxidative stress-related disease in a mammal in need thereof comprising administering an effective amount of a compound of formula (I) to the mammal, wherein R1-R4 and X1-X3 are as described herein. Examples of the oxidative stress-related diseases are a neurological disorder, a cardiovascular disorder, and a wound.
US7374909 mediated by receptors of the TNF/NGF superfamily of receptors; originally designated CBK, but now designated B1; DNA sequence: vector A B1 protein, its isoforms, analogs, fragments and derivatives, DNA encoding it and recombinant production are provided. The protein is useful in the modulation of intracellular inflammation, cell death and/or cell survival pathways.
US8372852 Purines as reverse transcriptase inhibitors Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders. In some embodiments, the enzyme inhibitors are compounds of formula (I) or a pharmaceutically acceptable salt or tautomer thereof:
WO2012069150A2 Cytoprotectant agents for the prevention of drug-associated side-effects The invention relates to cytoprotectant agents as medicaments for the prevention of drug-associated osteonecrosis of the jaw and/or the femur, to pharmaceutical compositions comprising a cytoprotectant agent and a bisphosphonate or denosumab, and to a method for the treatment or prevention of osteoporosis by the concurrent or subsequent adminstration of a cytoprotectant agent and a bisphosphonate or denosumab.
US7157596 Inhibitors of serine protease activity of matriptase or MTSP1 The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions ameliorated by inhibition of matriptase or MTSP1.
CN103445892A Vaginal stent containing methyl ester resin and diethylstilbestrol The invention relates to a vaginal mould containing methyl ester resin and diethylstilbestrol. The vaginal mould is composed of polymethyl methacrylate resin and the diethylstilbestrol according to the weight ratio of 20:(5-8) and has the advantages that contracture rate of the artificial vagina is greatly decreased by the aid of the vaginal mould containing estrogen. Since the vaginal mould capable of slowly releasing the estrogen is prepared by combining the polymethyl methacrylate resin with the estrogen, estrogen therapy is effectively combined with the treatment of the vaginal mould. Therefore, the vaginal mould with a slow-release function is of great potential in future clinical application.
EP2382974A1 Use of cyclosquaramide compounds as anti-tumour agents Use of squaramide-based macrocylic compounds as kinase inhibitors and as anti-tumour agents. More specifically, said compounds are used to treat diseases such as cancer, diabetes, neurodegenerative diseases, HIV replication, etc. Furthermore, the present invention likewise relates to pharmaceutical compositions that contain said compounds
US20100184847 Compositions for skin protection and improvement of skin diseases containing the dibenzo-p-dioxine derivatives The present invention relates to compositions for skin protection and improvement that contain dibenzo-p-dioxine derivatives as effective components. Since the compositions for skin protection and improvement that contain the dibenzo-p-dioxine derivative according to the present invention have excellent functions such as moisturizing and/or wrinkle prevention which are useful in prevention and improvement of various skin diseases, they can be extensively used as cosmetic ingredients or pharmaceutical agents for prevention and improvement of skin diseases.
EP1666053A1 Methods and compositions for stimulating neurite growth using compounds with affinity for fkbp12 in combination with neurotrophic factors The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound and a neurotrophic factor, such as nerve growth factor (NGF). The methods comprise treating nerve cells with the above compositions or compositions comprising the compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.
WO2008115088A8 Use of rhodamine 6g in the form of a medicinal agent for treating malignant neoplasms and amiloidoses Rhodamine 6G of chemical formula C28H3IN2O3-Cl is used as a medicinal agent 'OF7' for treating malignant neoplasms and amiloidoses at a dosage ranging from 1mg to 10g in the form of an aqueous, physiological or alcoholic solution For different purposes, the rhodamine G6 solution is orally administered before or after meals, or the rhodamine G6 solution is rectally administered or the rhodamine G6 1% solution is intravenously injected, or the rhodamine G6 is administered in the form of a suppository or a 1-5% ointment. The invented medicinal agent is widely used for treating oncological diseases and amiloidoses, is low toxic and does not produce side effects when it is used in pharmaceutically acceptable doses, makes it possible to reduce a treatment time and to enhance treatment efficiency.
US20080194526 Concentrate comprising a S1P receptor agonist selected from 2-amino-2-[2-(4-octylphenylethyl)]propane-1,3-diol, 2-amino-2-[4-(benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propane-diol, and 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}azetidine-3-carboxylic acid Disclosed is a concentrate for dilution comprising a S1P receptor agonist or a pharmaceutically acceptable salt thereof, propylene glycol and optionally glycerin. This formulation is adapted for patients in a difficult condition to swallow.
CN103169818A Powder for enhancing immunity of chickens The invention provides a powder for enhancing the immunity of chickens. The powder comprises the components of astragalus, semen plantaginis, honeysuckle, herba violae, chrysanthemum indicum, senecio scandens, wild buckwheat, red dates, dangshen, krestin, spatholobus suberectus, rhizome curculiginis and vitamins. The powder can be used for improving the disease resistance of a human body all around through improving or adjusting the functions such as humoral immunity, cellular immunity, nonspecific immunity and the like and also has the characteristics of convenience in processing, low cost, wide raw material source, nontoxicity and no residue, thus being very considerable in market prospect.
CN101219114B Pennogenin compounds solid state molecule dispersion preparation The invention relates to a special preparation form with pennogenyl saponin compounds as active components. The solid molecule pharmaceutical dispersion of the pennogenyl saponin compounds of the invention comprises 0.5 to 60 percent of pennogenyl saponin compounds and 40 to 99.5 percent of polyvinylpyrrolidone according to weight percentage. The invention has the advantages that the pennogenyl saponin compounds exist in a water-soluble solid phase carrier in the molecular disperse state with a dispersion degree up to 10 times less than nanosizing particles, and the invention can disintegrateand disperse quickly after entering the gastrointestinal tract and be absorbed by human body, thereby improving more than 2 times of biological availability. PVP series materials have very strong moisture absorption and disintegration property, and Polyxamer 188 and Myrij can further improve the quick-release property and enhance absorption. The preparation of the invention is mainly applied to gynaecological blood symptom comprising hemostasis, hematopoiesis and gynecological inflammation.
EP2260832A2 Optimal polymer mixtures for gastric retentive tablets Unit dosage form tablets for the delivery of pharmaceuticals are formed of the pharmaceutical dispersed in a solid unitary matrix that is formed of a combination of poly(ethylene oxide) and hydroxypropyl methylcellulose. The combination offers unique benefits in terms of release rate control and reproducibility while allowing both swelling of the tablet to effect gastric retention and gradual disintegration of the table to clear the tablet from the gastrointestinal tract after release of the drug has occurred.
CN103446160A Pharmaceutical composition containing cefoperazone sodium for injection and lidocaine hydrochloride injection The invention relates to a pharmaceutical composition containing cefoperazone sodium for injection and 2% lidocaine hydrochloride injection, and in particular relates to a combined application package, comprising cefoperazone sodium for injection and 2% lidocaine hydrochloride injection. When in a use, 2.8ml of sterile water for injection and 1ml of 2% lidocaine hydrochloride injection are added into each 1g of drug, to form solution with the concentration of 250mg/ml for intramuscular injection. The pharmaceutical composition not only has broad-spectrum antibacterial function but also can remarkably reduce local pain caused by the injection of cefoperazone sodium.
WO2012008782A2 Use of carbon nanotubes for preventing or treating brain disease The present invention relates to the use of carbon nanotubes for preventing or treating brain disease, and more particularly, to a composition for protecting cranial nerves, to a composition for preventing or treating neurodegenerative diseases or ischemic brain disease or to a composition for treating traumatic injuries to the central nervous system, containing carbon nanotubes as an active ingredient, to the use of carbon nanotubes for preparing a therapeutic agent for the abovementioned diseases and to a method for treating the abovementioned diseases. The composition of the present invention enables patients to recover from physical damage to the brain, exhibits superior efficacy for inhibiting the onset of Parkinson's disease and strokes in animal models for Parkinson's disease and strokes, and the cytotoxic effects of beta amyloid in beta amyloid toxicity tests. Therefore, the composition of the present invention can be effectively used in the preparation of medicine for protecting cranial nerves, therapeutic agents for preventing or treating brain disease, or therapeutic agents for treating traumatic injuries to the central nervous system.
CN103694089A Mailuoning phenol and preparation method and application thereof The invention relates to the technical field of medicines and provides a novel phenol compound, namely mailuoning phenol (1-(7-methoxy ethyl)-3,4-catechol), which has a function of treating cardiovascular diseases. The structural formula is as follows: FORMULA. The invention also relates to a preparation method for the compound which can directly inhibition increase NO release induced by LPS (lipopolysaccharide); the result is relevant to the activity of the mailuoning phenol to inhibition of LPS-induced RAW264.7 cells; the 0.1 MuM indometacin inhibition rate is up to 63.1 percent; the inhibition rate of the mailuoning phenol with the dosage of 0.625 muM is basically equal to the 0.1MuM indometacin inhibition rate and is up to 59.7 percent. Therefore, the mailuoning phenol is higher in anti-inflammatory activity and can be used for preparing a medicine for treating the cardiovascular diseases.
CN101095673B Application of 3-benzyl-5-(2-nitrophenoxymethyl)-gamma-butyrolactone The invention discloses the application of 3-benzyl-5-(2-nitro phenoxy)-gamma-butyrolactone as medicine that can inhibit cytoplasm vacuolization induced by chloroquinine. The medicine can inhibit cytoplasm vacuolization for vascular endothelial cells and smooth muscle cell, and its concentration is 60-180 um.
EP2767273A1 Death-associated protein kinases, inhibitors and activators thereof for use in pharmaceutical compositions and in predictive medicine The present invention concerns pharmaceutical compositions comprising DAPK or inhibitors or activators thereof in the treatment, prevention, amelioration and delay of cancer or in the induction or suppression of inflammation as well as predictive methods for determining the risk of developing cancer in a subject, for determining the overall and disease-free survival time of a subject suffering from cancer and for deciding a personalized therapy for a subject suffering from cancer. Further, kits in order to perform said predictive methods are described.
CN103751097A Ofloxacin vaginal swelling suppository, as well as preparation method and detection method thereof The invention relates to an ofloxacin vaginal swelling suppository, as well as a preparation method and a detection method thereof. The swelling suppository comprises ofloxacin, a drug-containing matrix formed by a matrix, and a swelling carrier, wherein an inclusion complex is formed by ofloxacin and beta-cyclodextrin, so that the solubility and stability of ofloxacin can be improved; the hygroscopicity of ofloxacin can be reduced due to addition of calcium glycerophosphate in the drug-containing matrix, and the stability of the suppository can be improved; the drug-containing matrix of the suppository further comprises a specific hardening agent. The ofloxacin vaginal swelling suppository provided by the invention adopts six original advanced technologies, is high in stability and durable in curative effect, and has the beneficial effects of preventing a liquid medicine from draining, avoiding secondary infection and the like.
CN103191083A Application of isorhapontigenin (ISO) to preparation of drugs with antitumor activity The invention discloses application of isorhapontigenin (ISO) to preparation of drugs with antitumor activity. The activity of the X-linked inhibitor of apoptosis protein (XIAP) is inhibited by lowering gene expression of the XIAP. Western-blotting, reverse transcription-polymerase chain reaction (RT-PCR), an adenosine triphosphate (ATP) bioluminescence detection method, chromatin immunoprecipitation (CHIP) and other methods are utilized to prove that the XIAP gene expression level can be obviously inhibited, then tumor cell apoptosis is induced and tumor cell proliferation is inhibited by pretreating various tumor cells with ISO, ISO can not obviously induce tumor cell proliferation and apoptosis, the endogenous XIAP gene is the effective target treated with ISO and ISO is used for specifically inhibiting gene expression of the XIAP. Experiments prove that ISO can effectively improve the sensitivity of chemotherapy drugs and promote tumor cell apoptosis and has extensive application prospects in foundation medicine, clinical treatment, new drug research and development and the like.
CN101385717A Solid dispersion containing sofalcone as active ingredient and preparation method thereof The invention provides a solid dispersion containing active ingredient of sofalcone and a preparation method thereof, the solid dispersion is characterized in that the solid dispersion is prepared by the active ingredient of sofalcone, a carrier material and a solubilizer; and the weight ratio of the active ingredient of sofalcone, the carrier material and the solubilizer is 1: 1-20: 0.01-2. The ratio of 1: 1-10: 0.01-1 is preferential. The carrier material of the solid dispersion is polyethylene glycol 1500, 4000 and 6000 preferentially; and the solubilizer contains 20-85 of polysorbate, 188-407 of poloxamer, glycerol, arginine and tris(hydroxymethyl) aminomethane preferentially. The solid dispersion can be prepared through the melting method, the coating method and the solvent-melting method.The solid dispersion can not only improve the dissolution rate, increase the in vivo absorption of rats and enhance the bioavailability, but also better solves the scale problem of the industrialization.
US20080095802 Targeted delivery of cytotoxic drugs A) to activated lymphocytes in patients iwth transplanted organs, B) as radiosensitizers to cancer cells in paients undergoing radiation therapy, and C) in vitaminpbinding proteins as drug carriers in the diagnosis and treatment of cancer This invention relates to the targeted delivery of cytotoxic drugs A) to lymphocytes responsible for the rejection of transplanted tissues, such as kidneys or hearts or bone marrow cells; B) the use of a non-toxic naturally existing delivery system to transport high concentrations of radiosensitizers to cancer cells; and C) to the targeted delivery of drugs in medical diagnosis and treatment of cancer.
US20090197831 Composition for the Treatment of Obesity and Hyperlipidemia Current invention is related to the pharmaceutical industry in general and to the industry of the manufacture of pharmaceutical products for weight reduction and hyperlipidemia treatment. The advantages of the current invention respect of the similar of the state of the art are that in the present invention side effects normally produced by the consumption of lipase inhibitors are eliminated; optimizing both the lipase inhibitor component and the fat-trapping; with the adequate composition of each one of the components and with very small amounts of each one. The invention consists of a composition for the treatment of the obesity and hyperlipidemia, characterized by comprising in combination a lipase inhibitor and a fat-trapping component.
CN102887869A Application of 3-acylamino-1,2,4-phentriazines to preparation of tumor sensitizer The invention relates to compounds which have a general formula (I), and pharmaceutically acceptable medicinal salt of the compounds which have the general formula (I), wherein R is defined in the specifications. The invention also discloses a preparation method for 3-acylamino-1,2,4-phentriazine derivatives, and a sensibilization effect of the 3-acylamino-1,2,4-phentriazine derivatives in the radiotherapy and chemotherapy of tumor.
WO2008139894A1 Nitrogenated aromatic 6-membered ring derivative, and pharmaceutical agent comprising the same Disclosed is a compound which has both of a neurite elongation activity and an angiogenesis enhancement activity, and which is applicable to the amelioration of a disease including a head injury or a central nervous system injury (e.g., spinal cord injury), cerebral infarction, an ischemic heart disease (e.g., cardiac infarction, organic angina) and a peripheral arterial disease (e.g., critical limb ischemia), or a sequela of the disease. Specifically disclosed is a compound represented by the formula (I). Preferably, in the formula (I), the group Nx represents an aromatic 6-membered ring having two nitrogen atoms; R0, R1 and R2 independently represent a hydrogen atom, an alkyl group, an amino group or the like; E represents an oxygen atom or a group -NR8 [wherein R8 represents an alkyl group or the like]; n represents an integer of 0 to 5; X and Y independently represent a bond, a cycloalkyl group, -CO- or the like; and Q represents a hydrogen atom or a phenyl group.
WO2010132580A3 Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15-A16-A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a -C(O)C1-C20alky or a diaminopropionic acid conjugated with a -C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.
CN1981779B Xanthosine composition and its production method A composite medicine for treating hepatism is prepared from scutelloside (60-2000 Wt portions) and glycyrrhizic acid or its pharmacologically acceptable salt (10-800). Its preparing process is also disclosed.
US20120114765 Anti-neoplastic compounds, compositions and methods Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
WO2009118748A1 Isoxazoline linked pyrrolo[2,1-c[1,4]benzodiazepine hybrids as potential anticancer agents and the process for preparation thereof The present invention provides compounds of general formula (5a-d) and (9a-h) useful as potential antitumour agents against human cancer cell lines. The present invention also provides a process for the preparation of pyrrolo [2,1- c][1,4]benzodiazepine hybrids of general formula (5a-d) and (9a-h).
CN1309666B Polymer composition of glucuronic acid glucosan A biocompatible intermolecular polymer complex comprises an anionic component and a non protein cationic component. The anionic component comprises a linear or branched polysaccharide chain wherein at least 5 % of the basic structural units are glucuronic acid. The cationic component comprises a linear or branched natural, semi-synthetic or synthetic oligomer or polymer.
WO2014151253A1 4-cyano-n-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2h-pyran-4-yl)pyridin-3-yl)-1h-imidazole-2-carboxamide for the treatment of hodgkin's lymphoma The present invention is directed to methods for the treatment of Hodgkin's lymphoma comprising administering to a patient in need thereof, a therapeutically effective amount of 4-cyano-N-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl)-1H-imidazole-2-carboxamide as mono-therapy or as combination or co-therapy with one or more chemotherapeutic agent or chemotherapy regimens.
CN103251636A Medicament for treating Candida infections and diseases caused by Candida, and preparation method thereof The invention relates to a medicament for treating Candida infections and diseases caused by the Candida, and a preparation method thereof. The medicament is characterized by using Asa tea saponin A as a raw material drug, wherein the Asa tea saponin A is a monomer substance separated from Camellia seed meal directly or from tea saponin compounds, and during preparation, stearic acid, glyceryl stearate, sesame oil, glycerol, triethanolamine, ethylparaben and water are used as base materials, the stearic acid, the glyceryl stearate and the sesame oil are used as an oil phase, and the glycerol, the triethanolamine, the ethylparaben and the water are used as a water phase. The Asa tea saponin A is firstly dissolved in a water phase, and then the water phase and the oil phase are mixed and emulsified into a cream. The medicament provided by the invention has good curative effects on the Candida infections and the diseases caused by the Candida, can inhibit or kill the Candida in superficial tissues and deep tissue organs, alleviates or eliminates inflammation, ulcers and other diseases caused by the infection, and is safe and nontoxic in use, simple in preparation technology and easy to operate.
US7015232 Stablizer retards cyclization and discoloration of quinapril The present invention is directed to ACE inhibitor-containing compositions stabilized by the presence of magnesium oxide. Preferably, the ACE inhibitor, quinapril, is protected from certain forms of degradation when prepared in a pharmaceutical composition consisting essentially of magnesium oxide as the stabilizing agent. The presence of magnesium oxide also lends itself to favorable processing conditions during the manufacture of ACE inhibitor-containing compositions, especially processing by wet granulation.
CN102836141A Composition capsule containing meptazinol hydrochloride, and preparation method thereof The present invention discloses a composition capsule containing meptazinol hydrochloride, and a preparation method thereof. Per 1000 composition capsules comprises 115.6 g of meptazinol hydrochloride, 14 g of pregelatinized starch, 5 g of carboxymethyl starch sodium, and 1 g of magnesium stearate. During preparation, the meptazinol hydrochloride is crushed and screened with a 80 mesh sieve; a prescription amount of the meptazinol hydrochloride is weighed, and is mixed with the pregelatinized starch and the carboxymethyl starch sodium; a proper amount of 70% ethanol is added to the mixed material to prepare a soft material; a 20 mesh sieve is adopted to carry out granulation; and the resulting wet granules are subjected to hot air drying at a temperature of 40 DEG C, and water content is controlled to less than 2%. The composition capsule of the present invention has advantages of simple production process, good drug taste, and convenient taking.
US20120083511 Crystalline (r)-(e)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1h-indazol-3-yl)vinyl)-1h-pyrazol-1-yl)ethanol The present invention provides crystalline (R)-(E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol useful in the treatment of cancer.
WO2012031045A3 Phosphonate ester derivatives and methods of synthesis thereof The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.
WO2007042421A1 Imidazo benzodiazepine derivatives The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5- d][1,4]benzodiazepine derivatives of the following formula (I) wherein the definition of substituents is described in the claims. It has been found that this class of compounds show high affinity and selectivity for GABA α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
CN101229176A Capsule capable of increasing bone density and improving menopausal symptoms The invention provides a capsule for increasing bone density and improving menopause symptoms; the invention is a healthcare food that takes calcium citrate, vitamin D and soybean isoflavone as the main raw materials. Proved by the functional test, the invention has the healthcare function of increasing the bone density.
US20080160004 Drospirenone, ethinylestradiol; oral contraceptives; kits The present invention relates to a pharmaceutical composition which comprises progestogens, preferably drospirenone, estrogens, preferably ethinylestradiol and 5-methyl-(6S)-tetrahydrofolate, can be employed as oral contraceptive and moreover prevents disorders caused by folate deficiency in the consumers, in particular cardiovascular disorders and, after conception of the embryo, congenital malformations caused by folate deficiency such as, for example, neural tube defects, ventricular valve defects, urogenital defects, and cleft lip, jaw and palate, without masking the symptoms of vitamin B12 deficiency, and at the same time even in the case of homozygous or heterozygous polymorphism of methylenetetrahydrofolate reductase facilitates unimpaired utilizability of the folate component 5-methyl-(6S)-tetrahydrofolate by the body and thus its biological activity for preventing the abovementioned congenital malformations caused by folate deficiency. In addition, a prolonged protective effect is maintained after discontinuation of the contraceptive.
WO2009089680A1 Method of modulating membrane potential of a cell Provided herein are methods of modulating membrane potential of a cell membrane using self-assembling compounds. Also provided herein are methods of regulating a natural voltage-dependent ion channel in a cell membrane using the self-assembling compounds disclosed herein. Further provided herein are methods of treating, preventing and /or managing a disease that is related to the abnormal membrane potential responses by using the self-assembling compounds disclosed herein.
CN103054852A Application of aphanamixoid A in preparation of medicament for resisting herpes virus The invention discloses an application of aphanamixoid A in preparation of a medicament for resisting herpes virus. Experiments prove that the aphanamixoid A has significant effects on resisting the HSV-1 (herpes simplex virus 1) and the HSV-2 (herpes simplex virus 2) and indicate that the aphanamixoid A has a potential application value in the field of treatment of herpes-virus infected diseases. Experiment references are provided for the application of the aphanamixoid A in the clinical treatment of herpes-virus infected diseases, certain guiding significance is provided to the preparation of the medicament for resisting the HSV-1 and the HSV-2, and the aphanamixoid A has important reference value.
CA2321254C Pyradazine derivatives having inhibitory activity against interleukin-1.beta. production Pyridazine derivatives represented by general formula (1) or salts thereof, wherein R1 represents lower alkoxy, lower alkylthio or halogeno; R2 represents H, lower alkoxy, lower alkylthio or halogeno; R3 represents OH, CN, halogeno, lower cycloalkyl, lower alkyl or lower alkenyl optionally substituted by an optionally substituted aromatic group or optionally substituted carbamoyl; R4 represents COOH, lower alkoxycarbonyl, optionally substituted carbamoyl, optionally substituted amino or optionally substituted ureido; and the broken line means a single bond or a double bond between the carbon atoms at the 4- and 5-positions. Because of having an excellent effect of regulating interleukin-1.beta. production, these compounds are useful as preventives/remedies for immunologic diseases, inflammatory diseases, ischemic diseases, etc.
CN103393637A Use of flavonoid compound in preparation of metabolic disease resistance medicines The invention belongs to the technical field of medicines, and relates to a use of a compound having a structure represented by formula (I), and concretely relates to a use of the compound (5aR,10aS)-5a,10a-dihydro-1,3,8,10a-tetrahydroxy-2,5a-di(3-methyl-2-butenyl)-11H-benzofuranyl[3,2-b][1]benzopyranyl-11-one in the treatment of metabolic diseases. The compound is separated from Morus nigra. Experiments prove that the compound has very strong adipocyte differentiation promotion, diabetic mouse insulin sensitivity increasing and blood sugar and blood fat reducing effects, and can be further processed to prepare insulin sensitizers, sugar reducing medicines and lipid reducing medicines which can be applied to the medicine field. The formula (I) is shown in the specification.
EP1248622B1 Pharmaceutical composition comprising a metabolite of buspirone 6-Hydroxy-8-[4-[4-(2-pyrimidinyl)-piperazinyl]-butyl]-8-azaspiro[4.5]-7,9-dione and its pharmaceutically acceptable salts and hydrates are useful in the allevation of anxiety.
CN202542107U Lansoprazole and hydrotalcite composition The utility model relates to an anti-ulcer medicinal composition. The composition is formed by packing two solid preparations, namely lansoprazole and hydrotalcite. Combined medication of the lansoprazole and the hydrotalcite is facilitated.
CN103044398A Crystal form of alfentanil hydrochloride The invention provides a crystal form I of alfentanil hydrochloride, wherein the crystal form belongs to a triclinic system, the space group is P-1, and the cell parameters are that: alpha=81.808(4) degree, beta=89.921(4) degree, gamma=70.217(5) degree, and Z=2. The crystal cell is the crystal form I of alfentanil hydrochloride prepared in the invention. The crystal form I of alfentanil hydrochloride obviously shortens the dissolving time of the product, makes sure the complete solution of crystal form I of alfentanil hydrochloride in a short time, and is in favor of the usage of a powder injection. Simultaneously, the crystal form substantially reduces the hygroscopic, and makes sure a lower water content, and the quality of the alfentanil hydrochloride is more stable in a pot life.
CN103145715A Macrocyclic carboxylic acids and acylsulfonamides as inhibitors of HCV replication The present invention provides compounds of the general formulas I-IX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The present invention further provides treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
US20100278810 Methods of Modulating Angiogenesis The present invention provides methods of modulating angiogenesis in an individual, the methods generally involving administering to an individual an agent that modulates the expression or activity of GPR124. In one embodiment, the methods of the invention relate to inhibiting pathological angiogenesis by decreasing activity of GPR124, which method may be carried out in conjunction with administration of one or more other anti-angiogenic agents.
CN1562042A Method for preparing long acting progestogen injection implant agent and use A slowly-releasing gestrinone injection for treating endometriosis by subcutaneous injecting or intramuscular injecting is prepared from biodegradable polymer PLGA or PLA as skeleton and gestrinon (R2323) as active component by solvent evaporation method.
EP1453820B1 Substituted 6h-dibenzo[c,h]chromenes as estrogenic agents This invention provides estrogen receptor modulators of formula (I), having the structure, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
US20070287632 Sulphur-Containing Oils For Controlling Plant Pathogens And Stimulating Nutrient Uptake The present invention relates to sulphur-containing oils, their preparation, and their use in controlling/killing plant pathogens and stimulating a plant's uptake of essential elements from the soil and to act as a soil pH adjuster.
CN102772806A Application of micromolecular nucleic acid miR-302 for treating or preventing testicular cancer The invention relates to endogenic non-coding microRNA (micro Ribonucleic Acid), a medicine composition containing the microRNA, and new application of the medicine composition for treating or preventing the testicular cancer. According to the invention, the microRNA belonging to the family member (miR-302) of the microRNA-302 and platinum-type anti-tumour medicines are utilized jointly, so that the treatment effect of the platinum-type anti-tumour medicines for the testicular cancer can be obviously improved, and simultaneously, the administration dose, the administration time course and the side effects of the platimun-type anti-tumour medicines can be reduced. The invention also improves a molecular mechanism of the platinum-type anti-tumour medicines for treating the testicular cancer and develops a new treatment target spot for treating the testicular cancer, thereby having a significant value.
US20100009900 2-{3-[2-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-1H-indol-4-yloxy} beta -D-glucopyranoside; sodium glucose transporter inhibitor; antidiabetic agent; Syndrome X, obesity, nephropathy, neuropathy, retinopathy, atherosclerosis, hypertension, ischemia, stroke, heart disease, irritable bowel disorder, cataracts Substituted indole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.
EP2101765A1 Use of epothilones in the treatment of osteoporosis and related diseases The present invention relates to the use of natural or synthetic Epothilones for the treatment prevention or alleviation of diseases caused by a dysbalance of osteoclast and osteoblast activity, especially osteoporosis.
WO2005027918A1 Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and a cyclooxgenase-2 inhibitor The present invention relates to pharmaceutical compositions end methods of treatment comprising administering to a patient in need thereof a combination of a 2 alkylidene-1 9-nor-vitamin D derivative and a cyclooxgenase-2 inhibitory or a pharmaceutically acceptable salt or prodrug thereof. Particularly, the present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof 2-methylene-19-nor-20(S) 1 a,25-dihydroxyvitamin D3 and a cyclooxgenase-2 inhibitor, or a pharmaceutically acceptable salt or prodrug thereof.
CN101134047A Smectite chewing tablet for treating acute and chronic diarrhea and gastritis and method of producing the same The present invention provides one kind of montmorillonite chewing tablet for treating acute and chronic gastritis and its preparation process, and belongs to the field of medicine preparation technology. The present invention includes the components and the preparation process of the medicine preparation. The montmorillonite chewing tablet consists of montmorillonite 1000-3000 weight portions, supplementary material 50-750 weight portions and corrective 3-11 weight portions. It is prepared through mixing the materials, adding water, alcohol or other wetting agent and pelletizing, and tabletting. Compared with available technology, the montmorillonite chewing tablet of the present invention has the advantages of reasonable recipe, simple preparation process, etc and is suitable for industrial production.
WO2008050987A1 Combination formulation with controlled release comprising metformin and glimepiride The present invention relates to a controlled-release metformin-glimepiride combination formulation, and particularly to a controlled-release metformin- glimepiride combination formulation for oral administration, where a controlled- release layer is constructed so that the release of metformin having high water solubility and high unit dose may be maintained for 24 hours by selectively designing a release-controlling material and an immediate-release layer is constructed so that the content of glimepiride having low water solubility and low unit dose may be maintained uniform and it may also be immediately released. In particular, a controlled-release metformin-glimepiride combination formulation herein may be embodied into a multi-layered tablet, where a controlled-release layer and an immediate-release layer are separated to completely separate metformin and glimepiride so that excipients constructing the controlled-release layer may not affect an rapid release of glimepiride, thereby minimizing the interaction of drugs and maintaining the complementary activities of the drugs, thus being efficacious for especially type 2 diabetes.
WO2006040666A1 Substituted n-alkylpyrimidinones This invention is directed generally to substituted pyrimidinone compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such substituted pyrimidinone include compounds generally corresponding in structure to the following formula (I): wherein R1, R2, R3, R4A, R4B, R4C, R4D and R4E are as defined in this specification. This invention also is directed to compositions of such substituted pyrimidinones (particularly pharmaceutical compositions), intermediates for the syntheses of such substituted pyrimidinones, methods for making such substituted pyrimidinones, and methods for treating (including preventing) conditions (typically pathological conditions) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.
WO2009140676A2 Compositions and methods for inhibition of retroviruses Described herein are methods and compositions for the inhibition of retroviral integration and replication. The methods and compositions inhibit the activity of one or more components of the SET complex or base excision repair enzymes and induce autointegration of retroviral double-stranded nucleic acid.
EP2062887B1 Aminopyridine derivative having aurora a-selective inhibitory activity Disclosed is a compound represented by the general formula [I] below or a pharmaceutically acceptable salt or ester thereof. (I) (In the formula, R1 represents a hydrogen atom, F, CN or the like; R1' represents a hydrogen atom or an optionally substituted lower alkyl group; R2 represents O, S, SO, SO2 or the like;R3 represents an optionally substituted phenyl group; X1, X2 and X3 independently represent CH, N or the like, provided that none or one of X1, X2 and X3 is N; and W represents a group represented by the following formula: , wherein W1, W2 and W3 independently represent CH, N or the like.)
CN102362866A Medicinal composition for treating diabetes and obesity The invention belongs to the technical field of medicinal preparations and particularly relates to a medicinal composition for treating diabetes and obesity and preparation and use thereof. The invention is characterized in that the active ingredient of a single dose of medicine comprises 10 to 90 milligrams of Sitagliptin or salt thereof based on Sitagliptin and 5 to 50 milligrams of Simvastatin or Lovastatin, preferably 25 to 50 milligrams of Sitagliptin or salt thereof and 5 to 25 milligrams of Simvastatin or Lovastatin. The medicinal composition can be prepared into any formulation acceptable in pharmaceutics, preferably oral solid preparation.
CN102093309A Novel crystal forms of Febuxostat and preparation method of novel crystal forms The invention belongs to the technical field of pharmaceutical chemistry, particularly relates to three crystal forms comprising H, I and J of 2-(3-cyan-4-isobutoxy)phenyl-4-methyl-5-thiazole formic acid (Febuxostat) and a preparation method of the three crystal forms. The invention also provides X-ray powder diffraction characteristic absorption peaks and infrared absorption peaks of the three crystal forms. The characteristic absorption peaks occur at the reflected angles 2 theta of about 6.71, 7.19, 10.03, 11.10, 12.96, 13.48, 15.78, 17.60 and 22.15 degrees in an X-ray powder diffraction pattern of the crystal forms. The invention further relates to a pharmaceutical composite containing the novel crystal forms and application of the novel crystal forms in preparation of medicaments for treating over-high uric acid-related diseases.
CA2223594C Myogenic differentiation of human mesenchymal stem cells Compositions of matter are provided which comprise a mixture of isolated muscle precursor cells with either isolated mesenchymal stem cells or isolated periosteum cells, optionally further including a myoinductive agent. Also provided are a method for inducing isolated human mesenchymal stem cells to differentiate into myogenic cells, a method for producing dystrophin-positive myogenic cells in a mammal with commitment muscle regeneration, and a use of the compositions for treating muscular dystrophy.
EP1436292B1 5-methoxy-8-aryl-¬1,2,4|triazolo¬1,5-a|pyridine derivatives as adenosine receptor antagonists The present application relates to compounds of the formula (I) wherein R1 is hydrogen, halogen or lower alkoxy; R2 is hydrogen or is C(O)- lower alkyl or -C(0)-phenyl, wherein the phenyl ring is unsubstituted or substituted by one or two substituents, selected from the group, consisting of halogen, lower alkoxy or trifluoromethyl, or is -C(O)-furanyl or -C(O)- thiophenyl, wherein the rings are unsubstituted or substituted by halogen; and to their pharmaceutically acceptable salts. The compounds may be used in the treatment of diseases associated with the adenosine A2 receptor.
WO2012139089A3 Fungal-derived carbohydrate-conjugated scaffold The present invention provides for compositions and methods for a purified fungal carbohydrate-linked polymer bead platform, which can serve as an artificial fungus-like particle to measure specific patient immune responses to fungal carbohydrate antigens. A specific embodiment comprises a purified β-1,3-glucan chemically conjugated to a polymer bead.
US20110052700 Gastric retentive pharmaceutical compositions for immediate and extended release of levosulpiride Gastric retentive oral dosage forms which provide both immediate and extended release of levosulpiride are described which may allow once- or twice-daily dosing. Methods of treatment using the dosage forms and methods of making the dosage forms are also described.
CN101919849A Enteric slow release preparation containing S-ketoprofen and S-omeprazole used as active components, as well as preparation method and application thereof The invention relates to an enteric slow release preparation containing S-ketoprofen and S-omeprazole used as active components, as well as a preparation method and application thereof. The S-omeprazole is an enteric pellet, and the S-ketoprofen releases a medicament through a slow release framework. The invention discloses the preparation method and the application of the enteric slow release preparation.
CN101074251A Azithromycin 4-phenproester derivative, its production and medicinal composition A compound with general formula (I), accepted additional salt formed of inorganic and organic acids, its production, medicinal composition and usage are disclosed. It belongs to azithromycin pentadecenic macrolide derivative, R1 represents hydrogen or acetyl or methane; R2 represents fatty hydrocarbon, substituted aromatic fatty hydrocarbon or substituted aromatic heterocyclic fatty hydrocarbon. It can be used to prepare medicines in treatment of bacterial infections.
CN101485628B Method for preparing long-acting ceftiofur suspension injection The invention provides a method for preparing long-acting ceftlofur suspendible injection. The injection comprises the following components in weight ratio of the injection are: 25 to 70 grams of hydrochloric ceftlofur, 2 to 15 grams of phospholipid, 2 to 15 grams of sorbitol high-level fatty acid ester, 0.1 to 1 gram of vitamin E and 1,000 milliliters of soybean oil for injection. The preparation method is characterized by comprising a process of dissolving the phospholipids, the sorbitol high-level fatty acid ester and the vitamin E in oil, adding the hydrochloric ceftlofur in a stirring state, grinding the materials to between 4 and 10 um through a colloid mill, encapsulating and packaging. The preparation method has the advantages that the method is simple to operate, long in efficacymetabolism time, can achieve effects identical with the repeated alternate injection of identical species of conventional dosage forms under the condition of injecting once, reduces operation frequency, saves labor and time, and reduces stress reaction.
CN1813817A Compound hedgehog hydnum dry-mixed suspension and its preparing method The present invention discloses a compound hericium dry suspension preparation. It is made up by using 600 g of hericium sporophore, 100 g of sucralfate, 50 g of magnesium trisilicate, 40 g of bismuth subnitrate, 5-15 g of polyvinylpyrrole, 50-160 g of lactose, 120-200 g of hydroxypropyl methyl cellulose, 2-6 g of Tween-80, 10-50 g of aromadenadrin powder and 3-15 g of sodium glutamate through the processes of pulverizing, granulating and filling. It has good therapeutic effect for curing ulcer of digestive tract.
US7351844 Adjust diffusion of oxygen; respiratory system disorders; cardiovascular disorders The invention relates to trans carotenoid salt compounds, methods for making them, methods for solubilizing them and uses thereof. These compounds are useful in improving diffusivity of oxygen between red blood cells and body tissues in mammals including humans.
WO2007068743A1 Use of polyunsaturated compounds as whitening agents The invention concerns the cosmetic or dermatological use of at least one compound of formula (I), wherein: R1, R2, R3, R4, R5 and G are such as defined in the description as whitening and/or depigmenting agents for the skin and/or hairs and/or the hair. The invention also concerns a cosmetic method for whitening and/or lightening the skin and/or hairs and/or the hair comprising applying a composition of the invention.
WO2009100282A1 Furo-and thieno[3,2-c] pyridines Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula (I), and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.
WO2006104280A1 Prophylactic/therapeutic agent for diabetes A 11β-hydroxysteroid dehydrogenase 1 inhibitor comprising a compound represented by the formula (1) or a salt thereof or a prodrug of the compound or salt. The inhibitor has an excellent activity and is useful as a prophylactic/therapeutic agent for diabetes, insulin resistance, obesity, a lipid metabolic abnormality, hypertension or the like. (1) wherein each symbol is as defied in the description.
CN102911235A Method for producing ursodesoxycholic acid by using chenodeoxycholic acid as raw material The invention relates to a method for producing ursodesoxycholic acid by using chenodeoxycholic acid as a raw material. The method comprises the steps of performing selective oxidation on the chenodeoxycholic acid to obtain 7-O-lithocholic acid; performing selective reduction on the 7-O-lithocholic acid to obtain the ursodesoxycholic acid containing a certain amount of the chenodeoxycholic acid; reacting the obtained ursodesoxycholic acid with a silicified agent to form ursodesoxycholic acid silicide which is insoluble in organic solvents, wherein the chenodeoxycholic acid contained in the ursodesoxycholic acid reacts with the silicified agent to form chenodeoxycholic acid silicide which is soluble in organic solvents; and acidizing and hydrolyzing the obtained ursodesoxycholic acid silicide to obtain a high pure ursodesoxycholic acid product.
EP2182936A2 Substrate reduction therapy The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.
WO2008104790A1 Salts of a selective beta-2 andrenoceptor agonist A pharmaceutically acceptable salt of 7-[(1R)-2-({2-[(3-{[2-(2-Chlorophenyl)ethyl]amino}propyl)thio]ethyl}amino)-1-hydroxyethyl]-4-hydroxy-1,3-benzothiazol-2(3H)-one provided it is not the ditrifluoroacetate, dihydrobromide or di-acetate salt; and the use of such a compound as a medicament (for example in the treatment of respiratory diseases (such as asthma or COPD).
US20120165363 Pharmaceutical Compositions Comprising Dextromethorphan and Quinidine for the Treatment of Neurological Disorders Pharmaceutical compositions and methods for treating neurological disorders by administering same are provided. The compositions comprise dextromethorphan in combination with quinidine.
US20110124577 Preparation for oral administration comprises quercetin glycoside and a water-based solvent extract of cartilage containing chondroitin sulfate It is an object of the present invention to provide a preparation for oral administration in which the bitter taste derived from quercetin glycoside is improved. The bad taste derived from quercetin glycoside can be improved, thereby improving palatability, by blending an aqueous chondroitin sulfate extract in a preparation for oral administration containing quercetin glycoside.
WO2014140988A1 Rifaximin for use in the treating of vaginal infections. This invention relates to rifaximin for use in the treatment of bacterial vaginal infections. The invention also relates to the use for treating infections characterized by the presence of bacteria that may be clindamycin and/or metronidazole resistant. The invention also relates to the use of rifaximin to treat patients with vaginal infections who have relapsed following prior treatment or who have bacteria resistant to antibiotics other than rifaximin.
US7737176 Substituted arylhexadienoic acids and esters thereof which can be used for the treatment and prevention of diabetes, dyslipidaemia and atherosclerosis, pharmaceutical compositions comprising them and processes for the preparation of them The invention relates to compounds of the formula I: and to the pharmaceutically acceptable salts thereof, to processes for the preparation of them and to pharmaceutical compositions comprising them, which are useful especially for the treatment and prevention of dyslipidaemia, atherosclerosis and diabetes.
WO2013178880A1 Composition for preventing headaches The present invention concerns a non-toxic solid pharmaceutical composition for oral administration, containing one or more cysteine compounds from the group of L-cysteine, D-cysteine and N-acetyl cysteine, combined with one or more additional active agents, at least one of which being selected from cystine, glutathione and methionine, the composition further containing one or more pharmaceutical additives. Further, the invention concerns a method for reducing the incidence of severe headaches, particularly migraine and/or cluster headaches.
CN102516299A S-Ornidazole phosphate amino acid salt, its preparation method and application The invention relates to an amino acid salt of S-Ornidazole phosphate, especially its monoamino acid salt. With a structural formula as shown in general formula I, the amino acid salt of S-Ornidazole phosphate is mainly used for treating anaerobic infections or protozoan infections.
US7329755 especially naphthalene sulfonamides, used for treating asthma Disclosed is an inhibitor of CCR8 that is represented by Structural Formula (I): Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a CCR8 inhibitor represented by Structural Formula (I). Also disclosed is a method of treating inflammatory disorders in a subject by administering a CCR8 inhibitor to the subject.
US20110059916 Methods and Compositions for Inducing Torpor in a Subject The present invention relates to the discovery the 5′-AMP and analogues thereof can be used to induce a state of torpor or suspended animation in subjects, as exemplified by studies carried out in laboratory mice. In these studies; mice were injected with high doses of 5′-AMP, which was found to result in a decoupling of the animals' body temperature regulation mechanism accompanied by a reduction in the animals' core body temperature, which tended to lower towards the ambient environmental temperature. It was further discovered that the introduction of high levels of 5′-AMP resulted in an induction of fat regulation genes such as procolipase (Clps) in tissues and organs that do not normally express Clps, this in turn was accompanied by a shift in metabolism from a primarily glycolytic energy metabolism (which is inhibited at lower temperatures) to one that relied primarily on the liberation and metabolism of free fatty acids. Substantial medical and other applications that arise out of this discovery are also disclosed.
CN102038654A Cetirizine hydrochloride orally disintegrating tablets and preparation method thereof The invention discloses cetirizine hydrochloride orally disintegrating tablets, which comprise the main drug of cetirizine hydrochloride and the auxiliary materials of mannitol, microcrystalline cellulose, hydroxypropyl cellulose, croscarmellose sodium, sodium bicarbonate, citric acid, saccharin sodium, magnesium stearate, talcum powder and essence. The cetirizine hydrochloride orally disintegrating tablets have favorable curative effect on allergic rhinitis, allergen-induced urticaria and pruritus, are convenient to take, can disintegrate rapidly, and provide convenience for the old people, children or patients who suffer from medicine-taking disorders or cannot fetch water conveniently.
CN101129332A Malotilate dry emulsion and method of preparing the same The invention provides a malouti-ester drying emulsion and making method, which comprises the following parts: 1. 00-60. 00 wt% malouti-ester, 1. 00-200. 00 wt% water-soluble high-molecular cohesive material, 1. 00-100. 00 wt% oil, 10. 00-1000. 00 wt% filling agent, wherein the water-soluble high-molecular cohesive material comprises polyvinyl alcohol or gelatin; the oil comprises Labrafac CC, Transcutol P, coconut oil, soya-bean oil, peanut oil or isopropyl myristate; the filling agent comprises maltodextrin, mannitol or cane sugar. The making method comprises the following steps: dissolving formulating amount of malouti-ester in oil; dissolving high-molecular cohesive material and filling agent in water; mixing the two liquid to stir or isotrope to produce emulsion; spray-drying or drying in frozen to emulsion to produce malouti-ester drying emulsion. The invention is surface active agent-free and preservative agent with better security in comparison with normal liquid emulsion, which is in dried powder or particles state with better stability.
US7592478 Ligand antagonists of RAR receptors and pharmaceutical/cosmetic applications thereof Novel ligand antagonists of the RAR receptors have the following structural formula (I): in which A is a CH2, CHOH, C═O or C═N—OH radical or a sulfur or selenium atom; B is a radical selected from among those of formulae (a) to (f): and Ar is a radical selected from among those of formulae (g) to (i):
WO2014151258A1 Substituted pyridine derivatives useful as c-fms kinase inhibitors The present invention is directed to substituted pyridine derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives in the treatment of disorders mediated by c-fms kinase. The present invention is further directed to a process for the preparation of said substituted pyridine derivatives.
CN101580526A Neamine-carboline carboxylic acid conjugate, preparation method thereof and application in medicine The invention discloses a neamine-carboline carboxylic acid conjugate, a preparation method thereof and application in medicine. In the method, carboline carboxylic acid and the derivative thereof are taken as a plane aromatic cluster structure and are conjugated with the neamine through a connecting arm to obtain the neamine-carboline carboxylic acid conjugate. Intercalation is carried out on a carboline ring, electrostatic and hydrogen bond interaction is carried out on the neamine, and the two interactions are complementary; the obtained conjugate has synergy effect and can strengthen the binding capacity with a target RNA. The in vitro antibiotic experiment result shows that the conjugate in the invention has good bacteriostatic activity and can be used as clinical potential antimicrobial agents; the invention measures the binding capacity of the conjugate in the invention and an HIV TAR RNA by adopting surface plasmon resonance; the experiment result shows that the conjugate in the invention has anti-HIV potential and can be used as a potential clinical anti-HIV preparation.
WO2007004733A1 ACTIVATOR OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR δ A compound represented by the general formula (II) below or a slat thereof is used as an activator of a PPAR δ. (In the formula, W3 represents a nitrogen atom or CH; Z1 represents an oxygen atom or a sulfur atom; R11 and R12 respectively represent a hydrogen atom, a halogen atom, an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, or an alkyl group substituted with a halogen atom and having 1-8 carbon atoms; R13 and R14 respectively represent a hydrogen atom of an alkyl group having 1-8 carbon atoms; A1 represents an optionally substituted pyrazole or a thiophene; and m represents an integer of 2-4.)
WO2009146802A1 Macrocyclic urea and sulfamide derivatives as inhibitors of tafia The invention relates to compounds of the formula (I) which are inhibitors of activated thrombin-activable fibrinolysis inhibitor. The compounds of the formula I are suitable for producing medicaments for prophylaxis, secondary prevention and treatment of one or more disorders associated with thromboses, embolisms, hypercoagulability or fibrotic changes.
EP2786985A2 Antagonists of the glucagon receptor The present invention provides for novel compounds of Formula I and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as their use in methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistence and hyperglycemia.
WO2011070253A8 Azabicyclo[3.1.0]hex-2-yl derivatives, method for preparing same, and pharmaceutical compositions containing same The invention relates to the compounds of formula (I), where: ALK is an alkylene chain, and W is a grouping of formula (II) or formula (III), where R and R' are as defined in the description. The invention can be used as a drug.
CN102348707A Pyrimidinecarboxamide derivatives as inhibitors of SYK kinase The compound of formula (I) or a salt, preferably a pharmaceutically acceptable salt, thereof; is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate mast cell activation, for instance allergic and inflammatory diseases, as well of potential use in cancer therapy, specifically heme malignancies.
CN102126993A Resveratrol derivative and application thereof to preparation of antitumor medicaments The invention relates to a resveratrol derivative. The resveratrol derivative is characterized by being shown as the structural formula in the specification. The invention also provides a medicament which comprises the resveratrol derivative and medicinally acceptable auxiliary agents and is used for treating cancers. The resveratrol derivative has remarkable inhibition effects on various tumor cell strains of lung cancer, lung adenocarcinoma, liver cancer, uterine cancer and the like; and toxicity to normal cells is obviously reduced.
EP1546137A1 Benzimidazol-1-yl-thiophene compounds for the treatment of cancer The present invention provides compounds of formula (I): (I) pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
CN102492009A Camptothecin 20- position cholic acid derivative and preparation method thereof The invention relates to a camptothecin derivative of the formula (I) and a medicine thereof, relating to a method for preparing the compound, in particular an application in treating a tumour using the compound as the medicine. R1 in the formula (I) is hydrogen and ethyl, and R2 is hydrogen and nitryl, and R3 and R4 are hydrogen and hydroxyl.
CN101903380A 5-aminocyclylmethyl-oxazolidin-2-one derivatives The invention relates to antibacterial compounds of formula (I) wherein one or two of U, V, W, and X represent N, the rest represent CH or, in the case of X, may also represent CRa wherein Ra is fluorine; R1 represents alkoxy, halogen or cyano; R2 represents H, CH2OH, CH2N3, CH2NH2, alkylcarbonylaminomethyl or triazol- 1-ylmethyl; R3 represents H, or, when n is 1, R3 may also represent OH, NH2, NHCOR6 or triazol-1-yl; A represents CR4; K represents O, NH, OCH2, NHCO, NHCH2, CH2NH, CH2CH2, CH=CH, CHOHCHOH or CHR5; R4 represents H or together with R5 forms a bond, or also R4 can represent OH when K is not O, NH, OCH2 or NHCO; R5 represents OH or together with R4 forms a bond; R6 represents alkyl; m is O or 1 and n is O or 1; and G is as defined in the description; and to salts of such compounds.
US20080103124 Cefdinir-containing pharmaceutical composition A pharmaceutical composition with an enhanced bioavailability, particularly improved an oral absorption, comprising cefdinir or a pharmaceutically acceptable salt thereof and aminoalkyl methacrylate copolymer E is disclosed.
WO2009115893A3 Novel 2 ', 2 ', 3 ', 3 ' -tetrasubstiuted nucleoside derivatives The present patent application relates to the novel nucleoside derivatives and novel intermediates, which are useful to antiviral, anti tumor and immunomodulatory activity, method of treating diseases, conditions and/or disorders modulated by viral infections with them, and processes for preparing them.
EP2619203A1 Tricyclic compounds, preparation methods, and their uses The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
US8697743 Antioxidant camptothecin derivatives and antioxidant antineoplastic nanospheres thereof The present invention is directed to antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs and the preparation of nanometer-sized camptothecin prodrugs. Methods of synthesizing the antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant camptothecin nanosphere prodrugs and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these antioxidant camptothecin nanosphere prodrugs for the preparation of delivery devices of other pharmaceuticals and/or drugs. Additionally, methods of treating cancer with the camptothecin and antioxidant derivatives of camptothecin analogs, and nanometer-sized camptothecin prodrugs are also provided.
WO2011049059A1 Composition comprising rna-enclosing carrier Provided is a composition comprising one or more kinds of RNA-enclosing carriers, said carriers being selected from among a monocyte, a macrophage and a shedding microvesicle originating in these cells. The RNA-enclosing carrier(s) in the aforesaid composition can maintain the RNA in a stable state in vivo.
US6858624 Comprises 5,8,14-triazatetracyclo(10.3.1.0.0)-hexadeca-2(11),3,5,7,9-penaene groups; for reducing drug addiction, treating Alzheimer's/Parkinson's diseases, and other nervous system disorders This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of nicotine addiction/withdrawal and CNS disorders.
CN1895340B Sobering-up composition A sobering-up composition is proportionally prepared from seabusckthorn fruit powder, pueraria root powder, VC and taurine.
EP1219595B1 O-anisamide derivatives o-Anisamide derivatives which serve as peroxisome proliferator-activated receptor (PPAR) agonists, in particular human PPAR agonists, and are efficacious in preventing and/or treating metabolic diseases in which they participate (hyperlipemia, diabetes, etc.), acid addition salts thereof and a process for producing the same. Namely, o-anisamide derivatives represented by general formula (1), pharmaceutically acceptable salts thereof and hydrates of the same, wherein R represents carboxy, carboxymethyl, CH2CHXCOY (wherein X represents mercapto or S(O)nMe wherein n is 0, 1 or 2; and Y represents amino or hydroxy).
US20060008574 Galactosyl isomalt, method for production and use thereof This invention concerns a method for preparation of galactosyl isomalt and galactosyl isomalt, the products and intermediate products that are obtained, and their use.
CN103755682A Novel crystal form for desloratadine and preparation method thereof The invention discloses a novel crystal form for desloratadine and a preparation method thereof. According to the novel crystal form for an antihistamine drug desloratadine, differential thermal analysis shows that a single absorption peak exists around 158 DEG C. The preparation method comprises steps of dissolving desloratadine into tetrahydrofuran, then dripping water into the system, after dripping, filtering to obtain filter cakes, and drying so as to obtain the crystal of the novel crystal form for desloratadine. The crystal form has high purity and good stability, has superiority in production, and can be reserved for a long time for preparation technology.
CA2599712C Folic acid-, vitamin b6- and vitamin b12-containing agents and the use thereof The invention relates to agents containing a folic acid, vitamin B6 and vitamin B12 and to the use thereof in hyperhomocystenemia for controlling homocysteine levels. The inventive agents are particularly suitable for preventive and acute treatment of vascular diseases of pregnant women and neurodegenerative diseases and are particularly advantageous in cases of hyperhomocysteinemia whose treatment with homocysteine level reducing agents causes secondary effects. Pharmaceutical agents and food supplements comprising the corresponding active substance combination, agents in the form of commercial packages containing corresponding combination preparations or monopreparations for a combined application are, in particular, also disclosed.
US7294652 Autoimmune conditions and NADPH oxidase defects The invention relates to methods and materials involved in diagnosing and treating autoimmune conditions. In particular, the invention relates to methods and materials involved in diagnosing arthritis conditions that are accompanied by an NADPH oxidase deficiency, methods and materials involved in treating, preventing, or delaying the onset of arthritis conditions that are accompanied by an NADPH oxidase deficiency, and methods and materials involved in identifying agonists and antagonists of NADPH oxidase activity.
CA2135639C Controlled release preparation containing a salt of morphine A new pharmaceutical preparation containing a number of coated particles comprising a salt of morphine coated with a barrier membrane providing a controlled, preferably pH-independent, release of morphine over the main part of the dose interval when administered once daily, providing a significantly reduced plasma concentration fluctuation compared to known morphine preparations. Also disclosed is a method for the manufacture of such a preparation and the use of such preparations for the manufacture of an analgesic useful in the treatment of severe chronical pain.
CA2396686C Transdermal therapeutic systems having improved stability and their production The invention relates to a transdermal therapeutic system (TTS). In said system, the formation of oxidative degradation products is reduced by at least one active ingredient which is contained in the system and can be oxidised by hydroperoxides during storage of the TTS. Said system is characterised in that the maximum sum of the peroxide numbers (PON), exhibited by the constituent parts of the formulation which contain the active ingredient(s) prescribed by the recipe for the TTS is 20. The invention also relates to a method for producing a transdermal therapeutic system of this type.
US20100278877 Body tissue filling material and method for production thereof There are provided a body tissue filling material having excellent engraftability and repairability, and a method for producing such a body tissue filling material in a simple manner. Specifically disclosed are: a body tissue filling material comprising a gelatin porous carrier, to the surface of which a coating having sulfated hyaluronic acid is applied; and a method for producing a body tissue filling material, comprising: a step (S3) of adding dropwise a sulfated hyaluronic acid solution to a gelatin porous carrier to effect impregnation thereof; a step (S4) of freezing the porous carrier impregnated with the sulfated hyaluronic acid solution; and a step (S5) of drying the frozen porous carrier.
US7041703 Particularly septic shock and/or autoimmune pathologies in which the aetiopathogenic role of inflammatory cytokines has been ascertained 2-Aminotetralines, a process for their preparation, and pharmaceutical compositions, for the prevention and therapeutic treatment of inflammatory pathologies (particularly septic shock) and/or autoimmune pathologies in which the aetiopathogenic role of inflammatory cytokines has been ascertained.
US20050165041 Combination for the treatment of airway disorders The invention relates to the combination of proton pump inhibitors and airway therapeutics for the treatment of airway disorders.
CN103585544A Pig growth promoting agent and preparation method thereof The invention discloses a pig growth promoting agent and a preparation method thereof, and belongs to the technical field of agricultural products. The pig growth promoting agent is prepared from the following ingredients in parts by weight: 5-22 parts of radix glycyrrhizae, 7-18 parts of parslane herb, 5-20 parts of radix puerariae, 5-10 parts of pericarpium citri reticulatae, 8-18 parts of radix platycodonis, 20-40 parts of flos caryophylli, 5-16 parts of tuber fleeceflower root, 20-30 parts of bulbus lilli, 11-19 parts of fructus amomi rotundus, 15-24 parts of fructus forsythiae, 13-26 parts of poria cocos, 6-18 parts of radix astragali, 7-19 parts of radix rehmanniae, 9-17 parts of folium isatidis and 20-40 parts of calcium carbonate. The pig growth promoting agent not only can effectively promote growth of the pig and improve the immunity of the pig, but also ensures that the pork of the pig fed with the pig growth promoting agent is harmless to people. The preparation method can effectively improve the effect of the growth promoting agent.
US6924295 Hetereocyclic amines such as 3-(5-(2-(2-(4-methylphenyl)-5-methyloxazol-4-yl)ethoxy)-1,2,3,4-tetrahydroquinolin-1-yl)propanoic acid ethyl ester, used as peroxisome proliferator activated receptor modulators; hyperlipemia; diabetis; A compound of formula (I) (wherein all symbols are as defined in the specification) and salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a compound of formula (I) have an activity of regulating peroxisome proliferator activated receptor regulator, the compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or treatment agent for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.
EP2108013A2 Crystalline forms of deferasirox The present invention provides novel crystalline forms of deferasirox, methods for their production, and methods for conversion of the novel forms to the known crystalline form I.
CN103070933A Winter healthcare foot washing solution and preparation method thereof The invention relates to a winter healthcare foot washing solution, which comprises the following raw materials: 1-10 parts of fructus kochiae, 1-15 parts of safflower carthamus, 1-15 parts of angelica, 1-15 parts of cassia twig, 1-10 parts of sappanwood, 1-100 parts of herba lycopi, 1-10 parts of polygala tenuifolia, 1-6 parts of boric acid, 1-6 parts of salicylic acid, 1-6 parts of alkanolamide and 1-6 parts of cocamidopropyl betaine. A preparation method for the winter healthcare foot washing solution comprises the following steps: 1) taking the fructus kochiae, the safflower carthamus, the angelica, the cassia twig, the sappanwood, the herba lycopi and the polygala tenuifolia, adding water for soaking, and decocting for two times each for 1.5 h; 2), filtering and concentrating a decocting solution into clear cream; and 3), adding boric acid, salicylic acid, alkanolamide and cocamidopropyl betaine into the clear cream. The winter healthcare foot washing solution has the effects of activating blood to remove blood stasis, dispelling cold to dredge collaterals, relieving swelling and pain, alleviating water retention, removing dirt, killing bacteria, protecting skin, treating tinea pedis and the like, and is simple to prepare and convenient to use.
WO2011125619A1 Intestinal protectant Disclosed is an intestinal protectant containing polyphosphoric acid or a pharmaceutically acceptable salt thereof as an active ingredient.
WO2009024221A1 6-thioxo-pyridazine derivatives Compounds of the formula I in which R1, R2 and R3 have the definitions stated in claim 1 are inhibitors of tyrosine kinases, more particularly of Met kinase, and can be used for purposes including the treatment of tumours.
CN101108171A Budesonide intestines sustained release dextromethorphan pellets and method of manufacturing the same The invention belongs to the technical field of medicinal preparation and relates to an enteric preparation and sustained or controlled release preparation, in particular to an enteric controlled release micro-granule with budesonide and its preparation method. The invention, which comprises a quick release celphere, a controlled release layer and an enteric layer, takes budesonide as active ingredient of the drug to coordinate with medicinal carrier supplementary materials. After the release level testing, it is proved that the enteric controlled release micro-granule, which adopts different enteric materials, controlled release material and different coating conditions, does not release in stomach but began to release slowly after entering the small intestine with even release level. Therefore, the enteric controlled release micro-granule in the invention can effectively prevent the release in stomach, ensure the slow release in small intestine and the release of drug in the affected section of small incestine, ileocecus and colon.
CA2819997A1 Preventive or therapeutic agent for pain associated with herpes zoster in acute phase Paroxetine, or a P2X4 receptor antagonist such as a diazepine dione derivative that is represented by general formula (IX) is used as a preventive or therapeutic agent for pain associated with herpes zoster in acute phase. (In the formula, R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, and the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, and the like, R4 and R5 represent a hydrogen atom and the like, and W represents a five- or six-membered ring heterocycle containing 1 to 4 nitrogen atoms as an element of ring that may have a substituent.)
US20090062281 such as 7-(2-[1,4']Bipiperidinyl-1'-yl-ethoxy)-6-methoxy-4-(4-phenoxy-phenylamino)-quinoline-3-carbonitrile, useful in the prevention of diseases associated with the Ras/Raf/MEK signaling cascade in a mammals, such as tumors, cancer, strokes, osteoporosis, arthritis and inflammatory diseases This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition of diseases associated with the Ras/Raf/MEK signaling cascade in a mammal, such as neoplasms, strokes, osteoporosis, cancer, rheumatoid arthritis, inflammatory disease, polycystic kidney disease, and colonic polyps, and methods of making the compounds of formula 1 and intermediates.
US20050129623 Inhalable aztreonam aerosol for treatment and prevention of pulmonary bacterial infections A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam, or a pharmaceutically acceptable salt thereof, delivered as an aerosol or dry powder formulation.
CN103007048A Ointment for treating blind pouches The invention discloses ointment for treating blind pouches. The ointment is prepared by grinding radix aconiti, coptis root, borneol, asarum, frankincense, crinis trachycarpi, common bletilla rubber and borax into powder, then sieving the powder with a 200-mesh sieve and mixing the sieved powder with monoglyceride uniformly. The ointment has the functions of contracting the blind pouches, resisting bacteria and diminishing inflammation and weakening anesthesia, can reduce swelling irritation of oral cavities of patients and promote healing of the blind pouches, is convenient to use and has an obvious effect.
US20110206656 Emergency interventions of active charcoal with dabigatran etexilate overdosing The invention relates to a method for treating an overdosing with active substance dabigatran etexilate of formula I optionally in the form of the pharmaceutically acceptable salts thereof, comprising the administration of an effective amount of charcoal.
WO2014035446A1 Methods and compositions for hypotensive resuscitation Methods of treating diseases and conditions wherein an improvement in cardiac output, organ perfusion, or tissue oxygenation are disclosed. The methods include treatments of diseases and conditions, such as hypovolemic shock, with an a2 adrenergic agent, like centhaquin and centhaquin citrate. The method utilizes an a2 adrenergic agent administered at low doses with a low volume of resuscitation fluid. Purified centhaquin and centhaquin citrate also are disclosed.
WO2013091082A1 Bis-(aryl/heteroaryl)-methylene compounds, pharmaceutical compositions containing same and their use for treating cancer The present disclosure relates to novel bis-(aryl/heteroaryl)-methylene compounds of formula (I) having vitamin D receptor agonist and histone deacetylase (HDAC) inhibitory efficacy as well as to methods for reducing or inhibiting the proliferation of cancer cells or for treating cancer cells.
CN102670624A Patch for treating rheumatic arthritis and preparation method thereof The invention discloses a patch for treating rheumatic arthritis and a preparation method thereof. The patch consists of a main medicament for treating rheumatic arthritis, a medicament solvent, a substrate and a penetrating agent, wherein the main medicament consists of triptolide and lidocaine serving as a pain-relieving medicament for relieving rheumatic arthritis pain. The patch is medical controlled-release slow release preparation, has a comprehensive pharmacological action, is used for blocking major development pathologic loops of the rheumatic arthritis disease, and has high specificity and a lasting pharmacological effect; and the preparation method is simple.
CN101062120A Medicine for curing waist and leg pain and its preparing method The invention relates to a pharmaceutical composition for treating waist and leg pains and process for preparation, wherein the medicament is prepared from wood louse, frankincense, myrrh, native copper, safflower, drynaria, rhubarb horsetails, borax and Chinese angelica root through steps of disintegrating, concentrating, granulating, and making capsule with pharmaceutically acceptable carriers or adjuvant.
US20080234187 In particular amidated, acetylated, phosphorylated and/or glycosylated derivatives; diagnostic agents including a nucleic acid or messenger RNA coding for the cytokine; isolated from human hemofiltrate Cytokine CC-1 having the amino acid sequence according to SEQ ID No. 6 and its biologically active fragments and/or derivatives, in particular amidized, acetylized, phosphorylized and/or glycosylized derivatives.
US20120294882 Modified tuberculosis antigens Modified Rv3616c proteins and their use as medicaments, particularly for the prevention of reactivation of tuberculosis.
US7470673 Using vector comprising nucleotide sequences coding atonal-associated polypetides as therapeutic tool in treating hearing impairment and inflammatory bone disorders; antiarthritic agents Compositions and methods are disclosed for the therapeutic use of an atonal-associated nucleic acid or amino acid sequence. Also, an animal heterozygous for an atonal-associated gene inactivation is also disclosed having at least one atonal-associated nucleic acid sequence replaced by insertion of a heterologous nucleic acid sequence used to detect expression driven by an atonal-associated promoter sequence, wherein the inactivation of the atonal-associated nucleic acid sequence prevents expression of the atonal-associated gene.
US7786108 Compounds and method for treating dyslipidemia Compounds of formula I wherein n, m, p, q, Y, R1 R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.
US20110065628 Medication Combinations for the Treatment of Alcoholism and Drug Addiction The present invention provides for the use of combinations of drugs to treat addictive disorders. More specifically, the present invention provides compositions and methods for treating disorders using combinations of drugs such as topiramate, ondansetron, and naltrexone.
EP1599480B1 Substituted hexahydropyrazino(1,2-a)pyrimidin-4,7-dion derivatives, method for the production and use thereof as medicaments The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidin-4,7-dion derivatives in addition to the physiologically compatible salts and physiologically functional derivatives thereof. The invention also relates to compounds of formula (I) wherein the radicals have the cited meaning, the physiologically compatible salts thereof and methods for the production thereof. The compounds can be used, for example, as anorectics.
CN102239164A 2h-chromene compound and derivative thereof Disclosed is a compound which has an excellent S1P1 agonistic activity and is particularly useful as an active ingredient for a prophylactic and/or therapeutic agent for diseases induced by undesirable lymphocyte infiltration or diseases induced by abnormal proliferation or accumulation of cells. Specifically disclosed are a 2H-chromene compound and a derivative thereof, each of which has an S1P1 agonistic activity and can be used particularly for the prevention and/or treatment of diseases induced by undesirable lymphocyte infiltration or diseases induced by abnormal proliferation or accumulation of cells.
CN103751151A Venlafaxine slow-release formulation capable of providing 24-h release result and preparation method of venlafaxine slow-release formulation The invention belongs to the field of pharmaceutical preparations, and discloses a slow-release formulation of venlafaxine hydrochloride. The formulation is composed of a piller containing venlafaxine hydrochloride and a slow-release coating layer attached in the outer layer; the preparation disclosed by the invention is capable of enabling a medicine to release continuously and stably within 24 h; steady blood concentration is kept; the drug administration frequency of patients is reduced; the drug administration safety and the patient compliance are improved; the preparation process is simple and practicable; the venlafaxine slow-release formulation disclosed by the invention is applied to industrial production.
US20080131372 Extruding mixture of alpha-2 adrenergic receptor agonist (brimonidine) and biodegradable polylactide Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to prevent the occurrence of one or more ocular conditions, or to reduce one or more symptoms of an ocular condition, such as an ocular neurosensory disorder and the like.
US20080249125 N-methyl-2-phenyl-2-{7-[2-(4-trifluoromethyl-phenyl)-ethyl]-4,7-dihydro-5H-thieno[2,3-c]pyridin-6-yl}-acetamide; sleep disorders The present invention relates to compounds of formula wherein R1, R2, R3, and R4 are as defined herein and hetaryl is a one or two ring-membered heteroaromatic ring system, connected to the carbon atoms of the piperidine group selected from the group consisting of or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders in which orexin pathways are involved, like sleep disorders.
WO2013017254A1 Oligosaccharides and oligosaccharide-protein conjugates derived from clostridium difficile polysaccaride ps-i, methods of synthesis and uses thereof, in particular as vaccines and diagnostic tools The invention relates to a synthetic oligosaccharide representing part of the repeating unit of the Clostridium difficile glycopolymer PS-I and having the sequence of the pentasaccharide a-L-Rhap- ( 1→3 ) -β-D-Glcp- ( 1→4 ) - [a-L-Rhap- ( 1→3 ] -a-D-Glcp- ( 1→2 ) -a-D-Glcp or a synthetic fragment or derivative thereof. Preferably, the claimed synthetic oligosaccharide bears at least one linker L for conjugation to a carrier protein or for immobilization on a surface. Further aspects of the invention relate to advantageous methods for synthesizing said synthetic oligosaccharide and oligosaccharide-protein conjugate as well as to uses thereof, in particular as vaccines and diagnostic tools.
US7683048 crystal form of 3-methylthiophene-2-carboxylic acid (6S,9R,10S,11S,13S,16R, 17R)-9-chloro-6-fluoro-11-hydroxy-17-methoxycarbonyl-10,13,16-trimethyl-3-oxo-6,7,8,9,10, 11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl ester; asthma, chronic obstructive pulmonary disease; dermatitis Polymorphic crystal forms of 3-methylthiophene-2-carboxylic acid (6S,9R,10S,11S,13S,16R, 17R)-9-chloro-6-fluoro-11-hydroxy-17-methoxycarbonyl-10,13,16-trimethyl-3-oxo-6,7,8,9,10, 11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl ester. The crystal forms possess anti-inflammatory activity and have very good stability. Methods for preparing the crystal forms are also described.
CN102432690A Application of Opuntia ficus-indica Milpa Alta polysaccharides to prevention and treatment of chronic neurodegenerative disease The invention discloses application of Opuntia ficus-indica Milpa Alta polysaccharides to the prevention and treatment of chronic neurodegenerative disease. The Opuntia ficus-indica Milpa Alta polysaccharides can improve the neurobehavioral disorder of rats, reduce the volume and cortices of cerebral infarction and the loss of hippocampal neurons, can reduce reactive oxygen species (ROS) in cells, has a good neuroprotection effect, can be taken as a medicine for preventing and treating chronic neurodegenerative disease of a central nervous system, and is used for preventing and treating chronic neurodegenerative disease of the central nervous system. The invention also provides an optimized process for extracting the Opuntia ficus-indica Milpa Alta polysaccharides. The extraction process has the characteristics of high polysaccharide yield and the like, is convenient, simple, economical and applicable, and is suitable for large-batch extraction.
WO2008123017A1 Novel diamide derivative Disclosed is a novel compound having a strong FXa inhibitory activity and exhibits quick, sufficient and lasting antithrombotic effect even by oral administration. Specifically disclosed is a compound represented by the general formula (I) below, a pharmacologically acceptable salt thereof or an FXa inhibitor containing any of them as an active ingredient. (In the formula, ring A represents a benzene ring; R1 represents a hydrogen atom, a halogeno group or the like; R2 represents a carboxy group, a carbamoyl group or the like; T1 represents a -C(=O)NH- group or the like; T2 represents a -CH2-CH2-C(=O)NH- group or the like; Q1 represents a tetrahydronaphthyridinyl group, a tetrahydrothiazolopyridyl group or the like; Q2 represents a single bond; and Q3 represents a phenyl group, a pyridyl group or the like.)
WO2013127917A1 New compositions for treating amyotrophic lateral sclerosis The present invention relates to compositions and methods for the treatment of amyotrophic lateral sclerosis. More specifically, the present invention relates to novel combinatorialtherapiesfor treating amyotrophic lateral sclerosisor a related disorder.
CN1951397B Physiological balanced nutrient with physiological balanced calcium The invention relates to a physiological balance calcium cooperativity nutrient which belongs to the health food production field. Having a coriaceous skeleton is the base of good health and a long life. In life of human, the sclerotin continually updates and recast. The cooperativity and the physiological equilibrium in various kinds of nutrient is the material base of recasting the coriaeous skeleton. After continuous long-term research and practice, the invention summarizes the international hypercalciuria calcium phylogeny and innovate the theory. And according to the four first-level element of recasting the coriaceous skeleton: 1.physiological equilibrium, which can prevent the bone trabecula losing and osteoporosis; 2.recasting the coriaceous bone matrix to prevent the biochemical harm; 3. the bone crystal coordinates with the osteocalcin to maintain normal calcification; 4. playing sports which is the essential condition of casting the highly qualified bones. The invention is to prepare the nutrient as required and distinguished different object and produce the series of products. The invention also innovates the productive technology, saves the equipment investment and improves the production efficiency about 50%.
CN102988285A Docetaxel injection composition and preparation method thereof The invention provides a docetaxel injection composition and preparation method thereof. The components of the docetaxel injection are as follows: the concentration of a main drug docetaxel ranges from 20 mg/mL to 60 mg/mL; the proportional range of the main drug to absolute ethyl alcohol is 1 : 1-1 : 50; the proportion of the main drug to poly(ethylene glycol stearate) 15 ranges from 1 : 1 to 1 : 50; anhydrous citric acid is used as a pH conditioning agent; and the pH range adjusted by anhydrous citric acid is from 3 to 4.5.
CN103181953A Medicine combination for preventing and curing piglets from diarrhea and preparation method thereof The invention discloses a medicine combination for preventing and curing piglets from diarrhea and a preparation method thereof. The diarrhea of piglets is a common and frequently-occurring disease in a pig farm. Currently, a method for preventing the piglets from diarrhea is that high-doses antibiotics and high-doses zinc oxide are added into feeding stuff. While the use of the high-doses antibiotics can cause immunosuppressant of the piglets, which is harmful to the growth of the piglets, and in addition, drug-resistant bacteria groups can be generated; and the adding of the high-doses zinc oxide can affect the palatability of the feeding stuff, and can pollute environment. The invention aims to replace the antiauxins to prevent the diarrhea of the piglets. The medicine combination comprises the components of zinc oxide and scutellaria extract powder, and is made into pellets after being subjected to enteric coating. After the enteric coating, the dose of the zinc oxide in the medicine combination can be greatly reduced; the zinc oxide avoids the chemical reaction with acid to directly arrive at small intestines, thereby playing the role of convergence diarrhea and preventing the piglets from diarrhea together with the scutellaria extract powder.
EP2477623A1 Compositions and methods for treating disorders of gastrointestinal motility Disclosed are methods of treating disorders of gastrointestinal motility by administering to a patient in need of such treatment a compound having formula (I).
CN101048081B Nutritional and/or pharmaceutical preparation for use in prophylaxis and treatment of disturbances in microelements absorption from the alimentary canal The invention dissolves the problem of the pharmaceutical preparation being a factor stimulating the absorption of microelements. The essence of the invention is that the preparation contains alpha-keto- glutarate or/and glutamine or/and glutamate or/and ornithine of alpha-keto- glutarate, dipeptide of glutamine and other amino acids or/and tripeptides of glutamine and other amino acids or/and glutamate with other amino acid or/and salts of alpha-keto-glutarate or/and glutamine or/and glutamate or/and ornithine of alpha-keto-glutarate, dipepetides of glutamine or glutamate with other amino acid in a dose 0.01-0.5 g/kg/day and administered orally stimulates the absorption of iron, zinc, copper, manganese, strontium, calcium, phosphorus and other microelements from the alimentary canal to the blood ensuring proper - physiological - curative level of these compounds in the blood of people and animals.
CN102210693A Method for preparing aspirin and dipyridamole multilayer tablets The invention provides a method for preparing aspirin and dipyridamole multilayer tablets, which is characterized by comprising: preparing dipyridamole sustained-release tablet cores by tabletting; and coating a stomach soluble insulation layer, an aspirin quick-release layer and a stomach soluble protective layer in turn. The method has the advantage that aspirin common release and dipyridamole sustained-release compound preparations are prepared by using conventional pharmaceutical equipment.
WO2014048894A1 Substituted indazol-pyrrolopyrimidines useful in the treatment of hyperfoliferative disorders The present invention relates to substituted indazol-pyrrolopyrimidinecompounds of general formula I: in which R1a, R1b, R1c, R1d, R2a are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
EP1967187A1 Composition based on rutin and L-lysine Composition comprises at least a rutine or its derivative and a L-lysine or its salt or ester. An independent claim is included for a pharmaceutical kit, preferably in the form of blister, comprising a first support, device, tablet or capsule containing the rutine or its derivative and a second support, device, tablet or capsule containing L-lysine or its salt or ester. - ACTIVITY : Antiinflammatory; Immunosuppressive; Dermatological; Antiarthritic; Neuroprotective; Antidiabetic; Ophthalmological; Antipsoriatic; Antiallergic; Nephrotropic; Gastrointestinal-Gen; Antiasthmatic; Gynecological; Respiratory-Gen; Antiparkinsonian; Nootropic. - MECHANISM OF ACTION : Arginase inhibitor. No biological data given.
US20120208847 Diagnostic and Therapeutic Alkyl Piperidine/Piperazine Compounds and Process Described herein are piperidine and piperazine compounds useful for treating neurodegenerated diseases characterized by a lack of dopamine neuron activity. The compounds are also useful for imaging dopamine neurons.
US7230023 Triazole compound containing a phosphonate group A triazole compound of the formula (I) or a pharmacologically salt thereof: wherein X represents a group of formula X—OH which has antifungal activity, L represents an -(adjacently substituted C6-C10 aryl)-CH2 group and R represents a —P(═O)(OH)2 group.
CN102048697A Method for preparing solid lipid nanoparticles of water-soluble anti-tumor medicine The invention belongs to the field of pharmaceutics and particularly relates to a method for preparing solid lipid nanoparticles of water-soluble anti-tumor medicine. The method comprises the steps of: dissolving stearic acid and lecithin in organic solvent, mixing, dropping anti-tumor medicine under the condition of water bath, stirring and slowly injecting polyanion sodium alginate so as to packing the medicine and the sodium alginate in nanoparticles, and acquiring the solid lipid nanoparticles by temperature changing, probe ultrasonic treatment and filter membrane treatment. In the invention, the adriamycin capsulated in the solid lipid nanoparticles is combined with the alginate so as to greatly increase the encapsulation rate, lower the absorption of surface medicine, and delay the release of the anti-tumor medicine for achieving the purpose of reducing the suddenly releasing of the medicine. Compared with the other method for increasing the encapsulation rate, the method provided by the invention is simple to operate, is low in preparing material demand and high in encapsulation rate, and can efficiently overcome multidrug resistance.
CN101862307A Bisulfate Cefdinir sodium capsule and preparation method thereof The invention provides a bisulfate Cefdinir sodium capsule and a preparation method thereof. The capsule is formed by taking bisulfate Cefdinir sodium as a main drug and taking a proper quantity of auxiliary materials, such as filler, disintegrating agent, lubricant and the like, and the auxiliary material sodium carboxymethyl starch and pregelatinization starch are dried and are respectively screened by an 80-mesh sieve with raw material bisulfate Cefdinir sodium. The capsule of the invention obviously changes the pharmacokinetics characteristics of Cefdinir and has the characteristics of high adsorption speed, large blood medicine density and high bioavailability. The capsule of the invention has stable quality, favorable aqueous solution, high dissolution, simple preparation technology and favorable feasibility and is suitable for industrialized production.
CN103301147A Nanometer compound ceftiofur suspension and preparation method thereof The invention discloses a nanometer compound ceftiofur suspension and a preparation method thereof, belonging to the technical field of antibiotic preparations for animals. The nanometer compound ceftiofur suspension comprises 1 to 30% of ceftiofur, 1 to 30% of astragalus polysaccharide, 0.1 to 40% of a surfactant, 0.1 to 30% of a wetting agent, 0.05 to 20% of a suspending agent, 0.1 to 10% of an anti-oxidant and 0.1 to 10% of an antiseptic, with the balance being soybean oil for injection. The nanometer compound ceftiofur suspension provided by the invention has the advantages of a scientific and reasonable formula, safety, high efficiency, a small particle size, uniform particle size distribution, simple preparation process, good stability and suitability for industrial mass production.
US20120022043 Pyrazolopyrimidine jak inhibitor compounds and methods The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.
CA2353962C Selective 5-ht6 receptor ligands Compounds which have enhanced affinity and selectivity for 5-HT6 receptors have been identified. These compounds can be used therapeutically in the treatment of mental disorders via administration in a pharmacologically acceptable delivery route to a patient in need thereof, or can be used to identify antagonists of 5-HT6 receptors by well known screening methodologies which could themselves be used in the treatment of mental disorders.
CN101439108A Medicament for treating postpartum tormina A medicine for curing postpartum tormina takes hawthorn, corydalis tuber, angelica, and brown sugar as raw materials. The hawthorn, the corydalis tuber, and the angelica are added with water to be decocted, and then added with the brown sugar to be dissolved, concentrated into paste, dried, crashed into medicinal powder, packed into capsules, and then sterilized, thus obtaining capsules. The medicine for treating postpartum tormina is characterized by precise effect and rapid healing without side effects and anaphylactic reaction, has positive roles in reducing disease of rate of controlling postpartum tormina and promoting health of women. Proved by clinical trial of 500 postpartum tormina patients, the medicine has 98 % cure rate.
EP1819720A1 A cost-effective process for preparation of manufacture of iron sucrose The present invention relates to a cost-effective process for manufacture of iron sucrose complex.
US20080176814 nonpeptidic inhibitors of cathepsin G; genetic diseases, degenerative diseases, DNA damages, neoplasia and/or skin diseases; DNA or polynucleotide sequences having a chain length of at least 60 nucleotides and being substantially not subjected to undergo efficient base pairing The present research is directed to the identification of non-peptidic inhibitors of cathepsin G characterised by high levels of selectivity and which can be efficaciously used in the treatment and prophylaxis of inflammatory occurrences and procoagulant conditions. The cathepsin G-inhibiting aptamers according to the invention consist of linear DNA or polynucleotide sequences having a chain length of at least 60 nucleotides and being substantially not subjected to undergo efficient base pairing.
US7662853 Monoacetyldiacylglycerol derivative for the treatment of sepsis The uses of mono acetyl diacyl glycerol derivatives extracted from deer antler for immunomodulating agent disclosed. Medical supplies and health foods containing the same as an effective ingredient also disclosed. Mono acetyl diacyl glycerol derivatives shows significantly effect for immuno modulation including immune enhancing. In the case of inducing cancer in a hamster by injecting cancer cell line, cancer development was delayed by activating lymphocytes, monocytes, and dendritic cells that are important factors to promote immunity and apoptosis of cancer cell was induced by promoting cytotoxicity of immune cell against cancer cell. Also in the case of mouse induced septic shock, it shows 100% survival rate even after lapse of 120 hours by control of immune function and suppression effect apoptosis. Therefore, mono acetyl diacyl glycerol derivatives according to the present invention can be effectively used for an immunomodulating agent, a sepsis treatment, a cancer treatment, and a health food for an immune modulation or the prevention of cancer.
CN101278897A Process for preparing brevifolin solid lipid nano particle The invention relates to a preparation method of brevifolin solid lipid nanoparticles; firstly, octadecanoic acid, lecithin and the brevifolin are dissolved in the absolute ethyl alcohol to form an organic phase solution; and the organic phase solution is placed into a pear-shaped flask to rotate and evaporate, so as to form an even organic phase membrane; and then the glycerine is dispersed in the distilled water to form the water phase by the stirring of thermostatical and magnetic force; the water phase solution is added into the flask and stirred to lead all lipid membrane in the organic phase membrane enter into the water phase by the wall of the flask, so as to form the milky mixed suspension which is processed ultrasonically and stirred to cool at room temperature, and mixed suspension system is obtained, finally the brevifolin solid lipid nanoparticles is obtained by freeze drying. The brevifolin solid lipid nanoparticles prepared by the preparation method of the invention not only is capable of improving the solubility and the stability of the brevifolin, but also more importantly has the advantage of targeting, thereby reducing dose, reducing the side effect and improving the bioavailability.
EP2178371A1 Heterocyclic modulators of cannabinoid receptors Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
EP1613303A1 Substituted p-diaminobenzene derivatives The present invention relates to aniline derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.
US20080207532 Use of Nordihydroguaiaretic Acid Derivatives in the Treatment of Drug Resistant Cancer, Viral and Microbial Infection Compositions and methods for using nordihydroguaiaretic acid (NDGA) derivatives for preventing the expression of MDR-1 gene and the synthesis of PgP protein or reversing multiple drug resistance in cells, and for using NDGA derivatives in combination with additional chemotherapeutic agents to treat drug resistant cancer and infections.
CN103356679A Application of Houttuynoid A in preparation of anti-platelet aggregation medicines The invention relates to an application of Houttuynoid A in preparation of anti-platelet aggregation medicines. The application of the Houttuynoid A in preparation of anti-platelet aggregation medicines provided by the invention is disclosed for the first time. As the framework type is a brand new framework type and the anti-platelet aggregation activity of the Houttuynoid A is unimaginably strong, the probability of giving any enlightenment by other compounds does not exist. The Houttuynoid A has remarkable substantial characteristics and meanwhile has remarkable progress for anti-platelet aggregation.
US20130029926 Compositions and methods for determing cancer susceptibility The invention generally relates to a molecular classification of disease and particularly to molecular markers for cancer susceptibility and methods of use thereof. More specifically, the invention relates to the determination, screening, or classification of an individual's genetic risk for breast and ovarian cancer susceptibility.
WO2014103475A1 Skin-exterior anti-ageing composition and production method therefor The purpose of the present invention is to provide a skin-exterior anti-ageing composition for preventing or improving trouble areas upon the exterior of the skin caused by ageing and degradation such as wrinkles, fine lines, blotches, and sagging. Accordingly, provided is a skin-exterior anti-ageing composition in which an aqueous medium is used as a base, and one or more selected from among L-ascorbic acid, derivatives thereof, and salts of the L-ascorbic acid and the derivatives thereof is included as an active ingredient.
US20120028963 Novel hydroxamate derivative, a production method for the same, and a pharmaceutical composition comprising the same The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives.
CN101785757A Taxol self-emulsifying preparation, preparation method and purpose thereof The invention discloses a taxol self-emulsifying preparation, a preparation method and the purpose thereof, belonging to the field of biomedicine. The taxol self-emulsifying preparation includes taxol, an oil phase and an emulsifier, wherein the oil phase contains fatty glyceride and the emulsifier contains PEGylated fatty glyceride. The specific combination of the oil phase and the emulsifier can ensure high stability of spontaneously-formed O/W (oil in water) micro emulsion after the self-emulsifying preparation is diluted by water, prevent the taxol dissolved in an emulsion drop hydrophobic core from being quickly separated out from the water, and make sure that micro-emulsion drops have centralized particle size distribution and controllable size; and the stability of self-emulsifying preparation diluent can be maintained for more than 24 hours. Without polyoxyethylene castor oil and ethanol, a product of the invention has the advantages of good safety, high stability, high medicine-loading quantity and simple preparation technique, and is applicable to industrial production.
EP2079469A2 Use of dipeptidyl peptidase iv inhibitors for preventing, delaying or reducing the occurance of edema A method to prevent, delay the progression or reduce, the occurrence of edema, comprising administering a therapeutically effective amount of a DPP-IV inhibitor, or pharmaceutically acceptable salt thereof, to a patient in need thereof.
WO2012033235A1 Pharmaceutical composition for treating anxiety disorder, containing n-acetyl-l-cysteine or derivative thereof The present invention relates to a composition for treating anxiety disorder, and more specifically, to a pharmaceutical composition for treating anxiety disorder such as posttraumatic stress disorder or phobia, containing N-acetyl-L-cysteine or a derivative thereof. In particular, according to the present invention, when N-acetyl-L-cysteine is administered during or after exposure therapy with respect to posttraumatic stress disorder and phobia, it is possible to block the relapse of fear memories for a long time.
WO2011099980A1 Use of the lactosylceramide synthase isoform b1, 4galt-v as a biomarker for cancer In one aspect, B1,4GaIT -V, an isoform of the enzyme lactosylceramide synthase, is provided as a biomarker for cancer. Also provided are methods and compositions directed at cancers characterized by the overexpression or upregulation of the lactosylceramide synthase isoform B1,4GaIT -V.
CN1785181A Gynostemma pentaphylla tolal glucoside dripping pills and its prepn. method A dripping pill of gynostemma pentaphyllumí»s heteroside is proportionally prepared from the active component (gynostemma pentaphyllumí»s heteroside) and the matrix (polyethandiol 4000 and hexadecanol) through dispersing the active component in fused matrix, dripping in atoleine, and condensing.
WO2010082600A1 Agent for maintaining healthy state of periodontal tissue comprising oleuropein and degraded product thereof Disclosed is an agent for maintaining the healthy state of the gum, maintaining the healthy state of the gingival, maintaining the healthy state of tissues that support teeth, preventing, treating or ameliorating periodontal diseases, maintaining the healthy state of periodontal tissues, or inhibiting the resorption of alveolar bones. Also disclosed are a food, a beverage, a composition for oral application, and a pharmaceutical composition, each of which contains an active ingredient having the above-mentioned activities. Specifically disclosed are an agent for maintaining the healthy state of the gum, an agent for maintaining the healthy state of the gingiva, an agent for maintaining the healthy state of tissues that support teeth, a prophylactic/treating/ameliorating agent for periodontal diseases, an agent for maintaining the healthy state of periodontal tissues, and an agent for inhibiting the resorption of alveolar bones, each of which comprises at least one component selected from oleuropein and degraded products thereof. Also specifically disclosed are a food, a beverage, a composition for oral application, and a pharmaceutical composition, each of which comprises any one of the above-mentioned agents.
US20080119496 7-Substituted Purine Derivatives for Immunosuppression The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula III:
US7199162 Pretreatment before allogenic transplantation of bone marrow or haematopoietic stem cells; may be administered with other chemotherapeutic or immunosuppressive agents; antitumor and anticarcinogenic agents The invention relates to the use of treosulfan as a conditioning agent before allogenic transplantation of bone marrow or haematopoietic stem cells, whereby treosulfan is administered, either as single effective agent, or in combination with other chemotherapetic agents or immunosuppressant agents.
CN102552234A Meclofenoxate hydrochloride medicinal composition and method for preparing freeze-drying powder injection of meclofenoxate hydrochloride medicinal composition The invention provides a meclofenoxate hydrochloride medicinal composition and a method for preparing a freeze-drying powder injection of the meclofenoxate hydrochloride medicinal composition. The meclofenoxate hydrochloride medicinal composition comprises the following components in part by weight: 30 to 100 parts of meclofenoxate hydrochloride, 60 to 120 parts of reduced glutathione and 40 to 80 parts of mannitol. The preparation method comprises the following steps of: a) dissolving the mannitol in water for injection, adding the meclofenoxate hydrochloride, and regulating the pH value to be 2-5; b) adding the reduced glutathione, stirring uniformly, adsorbing the solution by using 0.01 percent active carbon and filtering; and c) performing freeze drying to obtain the freeze-drying powder injection. The meclofenoxate hydrochloride medicinal composition has a reasonable formula and a good curative effect, and is high in quality stability, small in side effects and high in safety, and the adverse reaction of patients on medicine is reduced. The method for preparing the freeze-drying powder injection of the meclofenoxate hydrochloride medicinal composition is reasonable, reliable, simple, feasible, and suitable for industrial production.
EP1056458B1 Treatment of chronic pain Patients susceptible to, or suffering from chronic and/or female-specific pain are treated by administering an effective amount of a metanicotine-based compound.
US20050042655 Using hematopoietoic regulatory related polypeptide (HEMA) for use in diagnosis, treatment and prevention of hematopoietic disorders Disclosed are novel hematopioetic modulating nucleic acid sequences and polypeptides. Also disclosed are methods in which the nucleic acids and polypeptides are utilized in the detection and treatment of hematopoietic disorders.
US7115612 Arylsulfonamides as antiviral agents The present invention relates to novel sulphonamides of the general formula (I) in which the substituents R1, R2, R3, R4 and A and X are as defined in claim 1 and other claims, and also to processes for their preparation and to their use as antiviral agents, in particular against cytomegaloviruses.
CN101508712A Glucoside containing tetrazole structure, preparation method and application The invention relates to the diabetes-related drug field. More specifically, the invention relates to an sodium glucose transporter 2 (SGLT2) inhibitor containing a tetrazolylglucoside structure, a preparation method and application thereof to preparation of antidiabetic drugs, wherein, radicals are defined as the specification.
CN1814297A Acyclovir solubilization method in injection liquid This invention relates to a technique method that enhancing acyclovir dissolve in injection. In this invention acyclovir is dissolved in water or glucose water solution, poly sorbit ester 80, polyethylene glycol 400, are added in the injection, the content of acyclovir is 0.1-0.3%, content of poly sorbit ester 80 and polyethylene glycol 400 are both 2-8%. This invention resolves a problem that acyclovir doesní»t dissolve in water or glucose water solution or bring a lot of precipitations when temperature is lower than 20 degree centigrade, especially than 5 degree centigrade. So the defect of serious side effect of illness state delay can be avoided. poly sorbit ester 80 and polyethylene glycol 400 has solubilization character to make acyclovir more easily dissolve in water or glucose water solution, so the solubility of acyclovir can be greatly improved when temperature is lower than 20 degree centigrade, especially than 5 degree centigrade. So it is propitious to transportation, storage and using of acyclovir injection.
EP1390366B1 The citrate salt of 5,8,14,-triazatetracyclo(10.3.1.02,11.04,9)-hexadeca-2(11),3,5,7,9-pentaene The present invetion is directed to the citrate salt of 5, 8, 14-triazatetracyclo[10.3.1.0?2.11.04.9¿]-hexadeca-2(11),3,5,7,9-pentaene, formula 1, and pharmaceutical compositions thereof. The presetn invention is also directed to the various forms fo the citrate salt, particularly its hydrate and its anhydrous/nearly anyhydrous polmorph. The invention is also directed to processes for preparation of these citrate salt forms.
US20120184552 Latanoprost-containing aqueous eye drops and method for inhibiting adsorption of latanoprost to resin The invention provides an aqueous eye drop containing latanoprost, a surfactant, and an aliphatic mono- or di-carboxylic acid having a carbon number of 3-10 or a salt thereof. In addition, the invention provides a method of suppressing adsorption of latanoprost to a resin in an aqueous solution, by adding a surfactant and an aliphatic mono- or di-carboxylic acid having a carbon number of 3-10 or a salt thereof.
EP1681050A1 Dispersible sustained release pharmaceutical compositions Disclosed herein are pharmaceutical compositions, in particular, dispersible compositions comprising sustained release granules of at least one active pharmaceutical ingredient and at least one release retard hydrophobic polymer formulated with super disintegrant and lubricant, to achieve dispersible and sustained release effect.
EP2455081A1 S1P1 receptor agonists for use in the treatment of crohn's disease a S1P1 receptor agonist of formula (I), or a pharmaceutically acceptable salt, or solvate, or N-oxide, or stereoisomer or deuterated derivate thereof, for use in the treatment of inflammatory bowel disease, in particular Crohn's disease.
US20090036444 5-5-Membered fused heterocyclic compound and use thereof as HCV polymerase inhibitor The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
CN103494770A Veterinary pefloxacin mesylate injection and preparation method thereof The invention belongs to the technical field of preparation of veterinary drugs and in particular relates to a veterinary pefloxacin mesylate injection and a preparation method thereof. The veterinary pefloxacin mesylate injection comprises the following components of 1-10 percent (w/v) of pefloxacin mesylate, 0.05-1 percent (w/v) of complexing agent, 0.05-1 percent (w/v) of antioxidant, 1-50 percent (w/v) of pH buffer agent and the balance of thinning agent in the total 100 percent (w/v). Compared with the prepared injection in the prior art, the provided veterinary pefloxacin mesylate injection has the advantage that the drug quality is stable. Through long-term reserved sample observation and result comparison, the provided veterinary pefloxacin mesylate injection is stable in pH value and pharmaceutical effect, and the preparation method is feasible; therefore, the aim of the invention is well fulfilled.
US20100298339 [1,2,4]Triazolo[1,5-a]Pyridine and [1,2,4]Triazolo[1,5-c]Pyrimidine Compounds and Their Use The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.
WO2014030708A1 Preparation for preventing or treating type i diabetes The purpose of the present invention is to provide a preparation for preventing or treating type I diabetes, said preparation exerting an excellent effect of preventing or treating type I diabetes, and a method for preventing or treating type I diabetes. The onset and symptoms of type I diabetes can be very remarkably relieved by dosing a combination of: (A) at least one member selected from the group consisting of proinsulin, insulin, insulin A chain, insulin B chain, a fragment thereof and a variant thereof; with (B) α-GalCer.
CN102238957A Method and composition for enhancement of male erectile function Provided is a pharmaceutical composition for enhancing male erectile function comprising an erectile function-enhancing amount of an insulin-like growth factor selected from the group consisting of IGF-1 (Somatmedin-C) and analogue LR3 IGF1 in admixture with a pharmaceutically-acceptable diluents or carrier. Such compositions optionally further comprise compounds selected from an androgen, particularly, testosterone and dihydrotestosterone, a vasodilator, PDE5 inhibitor and prostaglandin E1.
EP1244641B1 Thiazolyl amide derivatives The invention relates to novel thiazolyl amide derivatives, to a method for producing them and to their use as medicaments, especially as antiviral medicaments.
US20110083201 Compositions for and methods of grazyme b inhibition The present invention is related to the discovery that serpina3n, a secreted protein, binds to and inhibits granzyme B activity. The invention thus provides cells that include a polynucleotide encoding a granzyme B inhibitory serpin, pharmaceutical compositions including a granzyme B inhibitory serpin or a polynucleotide encoding a granzyme B inhibitory serpin, methods for treating a patient in need of immunosuppression by administration of a granzyme B inhibitory serpin, and methods of transplanting cells (e.g., islet cells) expressing a granzyme B inhibitory serpin.
US7572833 E.g., N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal stabilized with a lipid; improved absorption and penetration; treating ischemia, immune diseases, Alzheimer's disease, osteoporosis, brain disorders, eye diseases, osteoporosis The present invention provides a preparation containing a compound of the formula (I) wherein R1 is an alkyl group having 1 to 4 carbon atoms or an optionally substituted aryl group having 6 to 10 carbon atoms; R2 and R3 are the same or different and each is hydrogen or an alkyl group having 1 to 4 carbon atoms, or R2 and R3 in combination form a ring having 3 to 7 carbon atoms; and R4 is a lower alkyl group optionally substituted by aryl, cycloalkyl or aromatic heterocyclic residue, or a pharmaceutically acceptable salt thereof together with a lipid. The preparation shows improved stability and improved absorption and penetration into tissue.
WO2010144499A3 Urea derivatives as kinase inhibitors The present invention is directed to novel ureas, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof which are useful for the treatment of protein kinases mediated diseases and conditions. The compounds of this invention have a general Formula (I) wherein R, R1 to R10 are defined herein.
WO2013173317A1 TREATMENT OF OBSTRUCTIVE SLEEP APNEA WITH α2-ADRENERGIC RECEPTOR AGONISTS This invention provides for methods, kits, and compositions for treating obstructive sleep apnea with one or more α2-adrenergic agonist (e.g. dexmedetomidine). The invention is also directed to modulating receptors in a patient suffering from obstructive sleep apnea by administering dexmedetomidine. One embodiment of the invention is a method of a treating obstructive sleep apnea with dexmedetomidine. The dexmedetomidine may be provided in a timed-release patch or a two-component composition having a quick release component and a timed-release component.
US20130053405 Carrier linked paliperidone prodrugs The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent Paliperidone carrier conjugate of formula (I) wherein Z0 is defined in the description and the claims as well as pharmaceutical composition comprising said compounds. The compounds are useful as medicament, especially for diseases or disorders which can be treated by Paliperidone.
US7488750 Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms The present invention provides novel forms of atorvastatin designated Forms VI, VIII, IX, X, XI and XII and novel processes for their preparation as well as processes for preparing atorvastatin Forms I, II, IV, V and amorphous atorvastatin.
US20090105188 Compositions and Methods for Treating Necrotizing Enterocolitis The present invention relates to a method for treating or preventing necrotizing enterocolitis (NEC) in a human neonate in need thereof, comprising administering to the neonate a pharmaceutically effective amount of a composition comprising a poly(ADP-ribose) synthetase/polymerase (PARP) inhibitor. Also contemplated herein is an infant food or treatment composition comprising a PARP inhibitor in an amount that is 5 to 500 times greater than a daily recommended intake dosage for the PARP inhibitor.
CN101602769A Podophyllum triazole derivants and application in preparing antiviral medicament and antitumor medicament The invention discloses podophyllum triazole derivants and application in preparing an antiviral medicament and an antitumor medicament. The podophyllum triazole derivants have a general formula shown as (I). The podophyllum triazole derivants have antitumor and antiviral activities.
CN102671201A Antibacterial nano silver modified polymeric micelle and preparation method thereof The invention belongs to the high-molecular nano biomedical materials, and specifically relates to a polymeric micelle in which the antibacterial nano silver is deposited at the core, and a preparation method of the polymeric micelle. Amphiphilic block copolymers form the micelle in a self-assembly manner through a direct dissolution method, and then, nano silver is generated at the core of the micelle in situ. The micelle has biocompatibility and also has certain temperature and pH sensitivity, the core-shell structure of the micelle can package multiple drugs, and simultaneously, with the existence of nano silver, the micelle has the curative effects of sterilization and bacterial inhibition.
CN103655519A Curcumin solid lipid nanoparticle with P-gp inhibiting effect and preparation method thereof The invention relates to a curcumin solid lipid nanoparticle with a P-gp inhibiting effect, and a preparation method and application thereof. The curcumin solid lipid nanoparticle comprises the following components according to mass ratio: 0.05-1% of curcumin, 5-15% of lipid material, 5-15% of an emulgator and the balance of water. According to the invention, the solid lipid nanoparticle technology is adopted to encapsulate curcumin, so that the stability of medicine is increased, the solubility of medicine is improved, the excretion function of small intestines is reduced, and the bioavailability of curcumin is improved. In addition, the preparation method of the curcumin solid lipid nanoparticle, disclosed by the invention, is the emulsification evaporation and low temperature solidification method which is simple and convenient and suitable for being used in a laboratory, and has low requirements for an apparatus.
EP1225878B1 Rar-gamma selective retinoid agonists for the treatment of emphysema This invention provides the use of RARη selective agonists for the manufacture of a medicament containing one or more such agonists for the treatment of emphysema and other diseases associated with alveolar damage. In another aspect, this invention provides the use of RAR agonists, preferably a RARη selective agonist for the manufacture of medicaments for promoting tropoelastin gene expression and alveolar matrix repair.
US20110177951 Microcapsules comprising active ingredients and a metal oxide shell, a method for their preparation and uses thereof The present invention provides a process for preparing microcapsules comprising a core material encapsulated by a metal oxide shell, microcapsules obtained therewith and uses thereof.
WO2013059837A3 Systems and methods for corneal cross-linking with pulsed light A method for controlling activation of Riboflavin applied to an eye includes applying the Riboflavin to a selected region of a cornea of the eye and initiating cross-linking activity in the selected region by activating the Riboflavin with pulsed light illumination. The pulsed light illumination has an irradiance, dose, and an on/off duty cycle. The irradiance, the dose, and the on/off duty cycle are adjusted in response to a determination of photochemical kinetic pathways for Riboflavin cross-linking activity and to control photochemical efficiency.
EP1975238A1 Gene construct, vector and dna vaccine for the vaccination of aquatic animals Improvements introduced in the object of patent application No. P200402093 relative to the immunisation of aquatic animals against infection caused by viral or bacterial pathogens or parasites, using DNA expression systems (vectors) that comprise a 5' enhancer sequence, a promoter and a nucleic acid sequence which encodes an immunogenic peptide of an aquatic animal pathogen. Optionally, the DNA expression system contains elements of a transposon, which, contrary to the vector used in said patent application, increases both the intensity and the duration of expression.
CN102327210B Vinpocetine suspension injection The invention discloses a vinpocetine suspension injection. The vinpocetine suspension injection is characterized by being mainly prepared from the following components in part by weight: 5 parts of vinpocetine, 2.5 to 20 parts of surfactant, 0.25 to 5 parts of antioxygen, and 2.25 to 60 parts of additive. The vinpocetine suspension injection is high in dissolvability, clarity, stability and bioavailability, and small in toxic and side effects, and can be used for hypodermic injection, intramuscular injection and intravenous injection. The vinpocetine suspension injection improves the qualityof preparation products and reduces toxic and side effects.
CN103214480A Pyrazolopyridines alkynylbenzene compound and medicinal composition and application The invention discloses a pyrazolopyridines alkynylbenzene compound having a structural characteristic shown in a formula (I) or its pharmaceutically acceptable salt or a stereisomer or prodrug molecules, and an application of the compound and its pharmaceutically acceptable salt or the stereisomer in preparation of medicines for treating or preventing tumor. Compared with a clinical used antitumor drug (imatinib), the compound has obvious advantage for resisting the activity of a plurality of tumor-derived type and drug resistance type cells, and the compound has the characteristics of good pharmacokinetics and low toxicity. The definitions of groups in the formula are disclosed in the specification.
CN101396532A Jingu Fengshi Hantong paste The invention discloses an analgesic bone rheumatoid plaster. The analgesic bone rheumatoid plaster has the functions of relaxing tendons, activating blood circulation, removing blood stasis, dispelling pathogenic wind, dispelling cold, removing dampness, stimulating the menstrual flow, activating collaterals, invigorating bone, relieving pain, resolving hard mass, and the like. The indications comprise bumps, fall injuries, pain on wounds, intercostal neuralgia, lumbar sprain, chest pain, pain in neck, shoulder, waist and lower extremities, rheumatism, rheumatoid arthritis, bone hyperplasia, bone spur, gout, bone fractures, neuropathic pain, and the like, and the efficacy is remarkable. The analgesic bone rheumatoid plaster is characterized in that the plaster can be directly pasted without heating when in application, and the paste oil can not be flowed anywhere and only leave a light mark, thereby not affecting the sanitation and not generating a wound surface on the skin by long-term application.
WO2006069182A3 THIENOISOQUINOLINE-PHENYLSULFONAMIDES AND THEIR USE AS ER-NFkB INHIBITORS This invention provides estrogen receptor modulators having the structure (I) wherein R1 to R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
CN103356838A Scorpion sting cream The invention discloses a scorpion sting cream and belongs to medical science. A folk remedy of nilgiri nettle for treating scorpion sting is low in swelling and pain relieving speed. The scorpion sting cream is prepared by taking the nilgiri nettle as a main ingredient. A specific implementation method is as follows: 10g of dry nilgiri nettle, 6g of cinnabar, 6g of realgar, 6g of bluestone, and 3g of musk are milled to fine powder, the powder is mixed with garlic paste, the obtained mixture is prepared into a lipstick type cream.
US20110020421 Biodegradable polyphosphazenes containing pyrrolidone side groups Biodegradable polyphosphazene polymers containing pyrrolidone side groups, and the biomedical use of such polyphosphazene polymers are disclosed.
WO2005118580A3 Tricyclic compounds as inhibitors of the hypoxic signaling pathway Tricyclic compounds that selectively inhibit HIF-lα activity are disclosed. Methods also are disclosed for reducing HIF-1α activity, and for inhibiting angiogenesis, tumorigenesis and/or metastasis, in a subject. In some embodiments, the tricyclic compounds surprisingly inhibit HIF-lα activity at non-cytotoxic concentrations, thereby avoiding drug side effects associated with significant cytotoxicity.
EP1333819B1 Inhalative solution formulation containing a tiotropium salt The invention relates to a propellant-free inhalation formulation of tiotropium bromide or tiotropium bromide monohydrate, which is dissolved in water or in a mixture consisting of water and ethanol, and to propellant-free inhalable aerosols resulting therefrom.
US20060251738 Rock flour, especially dolomite-based medicament, for the treatment of cancer diseases The invention relates to a drug for internal application, especially for the treatment of cancerous conditions. The drug comprises minerals, for example, silica flour, dolomite flour, quartz, calcium, magnesium powder, or combinations thereof. In a preferred embodiment the drug of the invention includes rock flour minerals with a grain size of from about 1 nm to about 150 nm. In certain embodiments, the rock flour drug of the invention optionally comprises at least one other ingredient, for example, an oil, an excipient, a carrier, and the like.
WO2006135254A1 Novel pharmaceutical composition and its use in a method for treatment of patients with upper respiratory mucosal congestion A PHARMACEUTICAL COMPOSITION ABSTRACT The present invention relates to a pharmaceutical composition including loratidine, its use in the treatment of upper respiratory mucosal congestion and a method of administration of the composition. Particularly, though not exclusively, the invention relates to a pharmaceutical composition including loratidine in an amount suitable for administration a maximum of 4 times a day, and a second active that is a hydroxyl-a-[(methylamino) methyl]-benzenemethanol, such 3-hydroxyl-a-[(methylamino) methyl]-benzenemethanol (phenylephrine), or salt thereof.
US20090131340 Use of flavonoids as immunomodulating or immuno-protective agents in cosmetic and dermatological preparations A method of treating or prophylactically treating immunosuppression or allergic and inflammatory symptoms of skin caused by UVB radiation which comprises applying to the skin a cosmetic or dermatological composition which comprises one or more flavonoids.
WO2011138977A1 Method of preventing or treating body weight-related disorders by employing vaspin Vaspin possesses an excellent anorexigenic effect and, accordingly, is useful for treating or preventing obesity or an obesity-related disorder. The anorexigenic effect of vaspin was effective in the obese subject with leptin resistance.
DE102005021382A1 Agent, useful to treat and prevent skin diseases e.g. psoriasis, preferably psoriasis of the palms and foot, nail psoriasis, neurodermatitis and atopic dermatitis, comprises zeolite, stinging nettle extract and further materials Agent, to treat and prevent skin diseases, comprises zeolite, stinging nettle extract and optionally further materials. An independent claim is included for the use of the agent as dietary supplement. - ACTIVITY : Dermatological; Antipsoriatic; Antiinflammatory. - MECHANISM OF ACTION : None given.
WO2009142588A1 Combination of (a) a chemokine receptor 1 (ccr1) antagonist and (b) glucocorticoid receptor modulator The present invention relates to a combination of (a) a chemokine receptor 1 (CCRl) antagonist and (b) a glucocorticoid receptor modulator. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treatment of airway diseases, such as chronic obstructive pulmonary disease (COPD) and asthma in mammals by administrating said combination. The invention also relates to a kit comprising the combination and use of said kit in treatment of airway diseases.
CN101317851A Freeze drying prescription containing glycyrrhizin and preparation method thereof The present invention discloses a prescription for freeze-drying product containing glycyrrhizin and the preparation method thereof, which pertain to the technical field of medicine. The prescription of freeze-drying product to which the present invention relates mainly comprises two parts of raw materials (glycyrrhizic acid monoammonium salt, cysteine hydrochloride and glycine) and auxiliary material (cosolvent, antioxidant and complexing agent); The preparation process mainly comprises four steps including liquid dispensing, adsorption of active carbon, filtration and freeze drying. The preparation process of freeze-drying product containing glycyrrhizin to which the present invention relates is easy in operation, simple in process, low in manufacturing cost, stable in product quality and convenient in transportation and storage, thus being allowable for use in combination with common clinical 5 percent of glucose injection and 0.9 percent of sodium chloride injection.
US20070092523 Combination Therapy Of Respiratory Diseases Using Antibodies Therapeutically effective anti-microbial compositions, useful especially against respiratory diseases caused or mediated by viruses, bacteria, and other respiratory parasites are disclosed, wherein said compositions comprise at least one neutralizing antibody, including high affinity antibodies, and an additional anti-infectious agent, such as an antiviral agent, for example, ribavirin, amantadine, rimantadine, or a neuraminidase-inhibitor. or antibacterial agents, including other antibodies. Also disclosed are methods of using such compositions to treat and/or prevent respiratory and related diseases.
US20100261679 CSF-1R, Inhibitors, Compositions, and Methods of Use Disclosed herein are compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof, compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.
CN101028380A Vegetable medicine for treating beri-beri A vegetative 'Jiaoqijing' for treating beriberi and smelly foot is prepared from 7 raw materials including pomelo peel, polyhexamethylene guanidine, carpesium root, tea tree, etc.
WO2009084275A1 Composition for oral administration Disclosed are: a composition which is highly safe and has an excellent effect of reducing a body fat and a neutral fat such as a visceral fat and a subcutaneous fat; and a food, a pharmaceutical preparation and a feed each comprising the composition. Specifically disclosed is a composition for oral administration, which comprises a carotenoid and a sphingolipid or a carotenoid and a flavonoid and/or a derivative thereof, preferably cryptoxanthin and a sphingolipid or cryptoxanthin and a flavonoid and/or a derivative thereof. Cryptoxanthin and/or the sphingolipid and/or the flavonoid may be derived from a citrus fruit. Preferably the citrus fruit is Unshu mandarin orange. The composition has an effect of reducing a body fat and/or an effect of reducing a neutral fat.
CA2295119C Use of a specific antagonist of 5ht2 receptors for preparing medicines useful for treating sleep-disordered breathing The invention relates to the use of a specific 5HT2 receptor antagonist for the preparation of medicines useful in the treatment of the sleep apnea syndrome.
CN101301282A Astaxanthin self-emulsifying soft capsule preparation and preparation thereof The invention discloses an astaxanthin self-emulsifying soft capsule preparation and a method for preparing the same, which relates to an astaxanthin preparation, in particular to the astaxanthin self-emulsifying soft capsule preparation capable of self-emulsifying in a body after oral administration as well as the method for preparing the same. The invention provides the astaxanthin self-emulsifying soft capsule preparation which has high bioavailability and good oxidation resistance and can self-emulsify in the body after the oral administration. The compositions of the astaxanthin self-emulsifying soft capsule preparation and the content by mass ratio are as follows: astaxanthin raw material: oil phase: emulsifier: coemulsifier is equal to 1: 20-60: 10-70: 0-30, wherein, an oil phase adopts natural vegetable oil or fatty acid ester, the emulsifier adopts nonionic emulsifier, and the coemulsifier adopts chain alcohol or short chain alcohol. The astaxanthin raw material, the oil phase, the emulsifier and the coemulsifier are added into a container, N2 is aerated into the container, and astaxanthin self-emulsifier is obtained by ultrasonic vibration; and the astaxanthin self-emulsifier is cooled to be the room temperature and is pressed to obtain the astaxanthin self-emulsifying soft capsule preparation.
US7276538 Composition and a method for treating hair loss The use of the polyamine known as spermidine, i.e., N-(3-aminopropyl) tetraminethylenediamine, as an active principle in the preparation of a composition for pharmaceutical or dietetic use in man for combating hair loss is disclosed.
US20090142334 DETECTION AND MODULATION OF IAPs AND NAIP FOR THE DIAGNOSIS AND TREATMENT OF PROLIFERATIVE DISEASE Disclosed are diagnostic and prognostic kits for the detection and treatment of proliferative diseases such as ovarian cancer, breast cancer, and lymphoma. Also disclosed are cancer therapeutics utilizing IAP antisense nucleic acids, IAP fragments, and antibodies which specifically bind IAP polypeptides.
US20080213374 Multi-kinase inhibitor, chemotherapeutics, pain relievers, anti-depressants, anti-inflammatories, ondansetron, nabilone, dronabinol, antibiotics, and antivirals; renal cancer; immune system; viral, bacterial infections; nausea; vomiting; pain; non-renal cancer; fatigue; skin irritation; bone marrow The present invention is directed to compositions comprising a nanoparticulate sorafenib, or a salt, such as a sorafenib tosylate, or derivative thereof, having improved bioavailability. The nanoparticulate sorafenib particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the treatment of cancer, renal cancer, and related diseases.
CN101422507A Combination of baicalin and atractylodes macrocephala lactone and preparation method thereof The invention discloses a combination which contains baikal skullcap root and atractylodes and is extracted from drug ingredients of baikal skullcap root and atractylodes. The combination also contains scutelloside and atractylodes lactone (I, II, III), wherein, the mass percent of the baikal skullcap root is 13 to 27 percent while the mass percent of the atractylodes lactone (I, II, III) is 0.5 to 2 percent. The preparation method of the combination can be a method of ethanol water hot reflux extraction added with large-hole resin and can also use a supercritical extraction method. The medical combination can be prepared by taking baikal skullcap root and atractylodes extract as drug action components and adding with pharmaceutic adjuvant acceptable in medical science or a medicine preparation can be prepared by a monomer, which can be used for curing and/or preventing fetal irritability and for protecting fetuses.
WO2008146710A1 Skin whitening agent Disclosed are: a skin whitening agent comprising, as an active ingredient, a complex of carbonic acid and/or bicarbonic acid, a metal and an LF, a decomposition product of the complex, or a complex of carbonic acid and/or bicarbonic acid, a metal and a decomposition product of an LF; and a food, beverage, feed or cosmetic comprising the skin whitening agent. The skin whitening agent can be ingested safely on a daily basis, and exhibits an excellent skin whitening effect.
US20130053368 Methods for treatment of parkinson's disease New uses of safinamide, safinamide derivatives and MAO-B inhibitors in novel types of treatment for Parkinson's Disease are described. More specifically, the invention relates to methods for treating Parkinson's Disease through the administration of safinamide, a safinamide derivative, or a MAO-B inhibitor, in combination with other Parkinson's Disease agents or treatments, such as levodopa/PDI or dopamine agonists.
CN102166205A New medical application of paeonol and derivatives thereof The invention relates to new application of paeonol and derivatives thereof in the pharmacy field. The animal experiment research shows that paeonol and derivatives thereof can obviously relieve or eliminate the inflammatory reaction of the local tissue of the eye with immunologic conjunctivitis, obviously reduce the infiltration of acidophilic cells and the degranulation of mast cells in the conjunctiva tissue, obviously relieve the inflammatory reaction of the anterior segment of the eye with uveitis, reduce the infiltration of inflammatory cells in the vitreous body and retinal tissue, effectively control the non-infectious immune inflammation of the dry eye, and obviously relieve the inflammatory reaction of the animal model eye with chronic conjunctivitis; and the clinical experiment research shows that the paeonol can be used for effectively treating eye diseases such as sclerotitis and the like. The invention provides a medicament for treating eye diseases, which has the advantages of exact curative effect and wide source and is safe and convenient; and the medicament can be combined with one or more pharmaceutically acceptable carriers or excipients to be prepared into a pharmaceutical composition or preparation of the paeonol and derivatives thereof.
CA2547378C Edible compositions which are adapted for use by a companion animal Disclosed herein are a variety of embodiments of compositions and methods which are each adapted for use by a companion animal. In one embodiment, an edible composition comprising an amount of a soluble mineral component is disclosed, wherein the soluble mineral component comprises one or more minerals selected from the group consisting of zinc, manganese, tin, copper, and mixtures thereof, wherein the amount is an effective amount for use as an oral medicament. In further embodiments, a phosphate component is included. The edible compositions are advantageously companion animal foods or supplements. Further disclosed are methods selected from treating oral cavity tartar, oral cavity plaque, periodontal disease, gingivitis, breath odor and combinations thereof comprising orally administering a described composition to a companion animal.
WO2006119300A3 Method of using oxidative reductive potential water solution in dental applications Methods of using oxidative reduction potential (ORP) water solution that is stable for at least twenty-four hours in dental applications are provided. The ORP water solution can be administered to patients for the routine disinfection of the oral cavity as part of an on-going program of oral hygiene. The ORP water solution can further be used to irrigate and/or disinfect oral tissues and surfaces during dental procedures, oral surgery, or maxillo-facial surgery. Also, the ORP water solution can be administered to treat patients with damage to the oral tissues caused by disease or surgery.
WO2010113801A1 Tooth calcification agent and method for producing same A tooth calcification agent which comprises tetracalcium phosphate particles (A) and an alkali metal phosphate (B), characterized in that the content of the tetracalcium phosphate particles (A) is 1 to 80 parts by weight per 100 parts by weight of the total tooth calcification agent, and the content of the alkali metal phosphate (B) is 0.5 to 50 parts by weight per 100 parts by weight of the tetracalcium phosphate particles (A). Thus, a tooth calcification agent having an excellent calcification effect, in particular an excellent calcification effect on the surface of the enamel, is provided.
US20100267749 Trisubstituted furopyrimidines and use thereof The invention relates to the novel 4,5,6-trisubstituted furo[2,3-d]pyrimidine derivatives of formula (I), to methods for their production, their use in the treatment and/or prophylaxis of diseases and their use in the production of drugs for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases.
WO2006059714A1 Composition for prevention and/or treatment of bone diseases, physiologically functional or health foods containing the composition, and medicinal preparations containing the composition as the active ingredient The invention aims at providing medicines or physiologically functional or health foods which contain phenylpropanoid dimers resulting from natural products as the active ingredient and which have preventive and/or therapeutic effects against bone diseases. The invention provides medicines and physiologically functional or health foods containing at least one compound represented by the general formula (I) or a physiologically acceptable salt or hydrate thereof: (I) wherein R'1, R'2 and R'3 are each independently hydrogen, hydroxy, or alkoxy of 1 to 3 carbon atoms; and R1, R2 and R3 are each independently hydrogen or alkenyl of 3 to 5 carbon atoms.
WO2007109088A2 Combinationtherapies of thiazolidinedione analogues and glucocorticoid agonists The present invention relates to thiazolidinedione analogues that are useful for treating inflammatory disease.
CN1660104A Enteric coated tablet of glipizide and preparation method An enteric tablet of glipizide for treating the diabetes B is proportionally prepared from glipizide and proper auxiliaries.
WO2012011081A1 Derivatives of oxadiazole and pyridazine, their preparation and their application in therapeutics The invention relates to compounds of formula (I): in which: n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a -CH- group; X1 represents a nitrogen atom or a -CH=CH- group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; one of X1, X2, X3 being other than a nitrogen atom, X2 and X3 not being an oxygen atom at the same time; R1, R2 are absent or represent, (i) independently of one another, a hydrogen atom or a (C1 -C4)alkyl group, (ii) R1 and R2 may form, with the carbon atom to which they are attached, a -(C3-C10)cycloalkyl- group; Y represents a -(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom or a (C1 -C6)alkoxy group; Z1 is absent or represents an -NH- function; Z2 and Z3 are as defined in the description. The invention also relates to a process for preparing compounds of formula (I), compositions containing them and their application in therapeutics.
US20120053144 Cobalamin Taxane Bioconjugates For Treating Eye Disease The present invention is directed to methods of treating eye disease. In one embodiment, the method can comprise administering a bioconjugate to a subject to treat the eye disease, where the bioconjugate comprises a taxane covalently bonded to a cobalamin. Additionally, the bioconjugate can be dissolved in an aqueous solution prior to administration.
US20100069877 Apparatus and method to dispense hpc-based viscous liquids into porous substrates, e.g., continuous web-based process Systems and methods are provided for dispensing compositions comprising sols, sol-forming compounds, or highly viscous compositions into porous substrates. In some embodiments, the porous substrates are elements of transdermal delivery devices. In some embodiments, the highly viscous compositions comprise alkylcellulose ethers, or derivatives thereof, in particular, hydroxypropyl cellulose. Such may be useful in continuous web-based manufacturing processes.
US20110207764 Cyclopolysaccharide compositions The present invention is directed to a composition including: (a) an active ingredient other than bendamustine; (b) a charged cyclopolysaccharide comprising at least one charged group; and (c) a stabilizing agent comprising at least one charged group having a charge opposite to that of the cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma which contain entities (such as enzymes, other proteins and the like) and/or conditions which can decompose or deactivate the active ingredient.
WO2014118097A1 Compositions comprising 15-ohepa and methods of using the same The present invention relates to the compositions, formulations and methods of treating fatty liver disorders, such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) and their sequelae by administration of 15-OHEPA.
EP2606888A1 Trpm8 antagonists The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula: Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, inflammatory conditions and urological disorders.
US7015347 Stable no-delivering compounds Disclosed are novel NO-releasing compounds which comprise a stabilized S-nitrosyl group and a free alcohol or a free thiol group. Also disclosed is a method of preparing the NO-releasing compounds. The method comprises reacting a polythiol or a thioalcohol with a nitrosylating agent. Also disclosed are medical devices coated with the disclosed compounds, methods of delivering NO to treatments sites in a subject by utilizing the medical devices and methods of sterilizing surfaces.
CN101116669A 20(R)-ginsenoside composition and uses thereof The invention relates to a combination made of 20(R)-ginsenoside taken serving as active constitutent and the application of the combination as medicine or health products. The 20(R)-ginsenoside combination mainly comprises the following weight percentage compositions of the components: 30 percent to 60 percent of 20(R)-ginsenoside Rg3, 10 percent to 40 percent of 20(R)-ginsenoside Rh2 and 10 percent to 30 percent of ginsenoside III, wherein the ginsenoside III is 20(R)-protopanoxadiol-3-O-beta-pyrane xylopyranosyl (1-2) beta-D-pyrane glucosyl (1-2) beta -D-pyrane glucoside. The invention relates to application of the drug combination in preparing anticancer aided drug for preventing and curing leucocyte reduction caused by radiotherapy and chemotherapy and in medicine or health products improving human body immunity.
WO2011087051A1 Therapeutic agent for atherosclerosis comprising s1p2 receptor antagonist Disclosed is a therapeutic agent for atherosclerosis. The therapeutic agent for atherosclerosis comprises an S1P2 receptor antagonist as an active ingredient.
CN102349899A Application of sophocarpine to preparation of medicament for treating respiratory system diseases caused by coxsackie virus B The invention discloses application of sophocarpine or pharmaceutical salts thereof to preparation of medicament for treating respiratory system diseases caused by coxsackie virus B. The sophocarpine or pharmaceutical salts thereof can be used as medicaments for treating viral pneumonia and bronchitis disease caused by the coxsackie virus B. According to the sophocarpine or pharmaceutical salts thereof, the cure rate can be improved, the death rate can be reduced; and the sophocarpine or pharmaceutical salts thereof have no obvious toxic effects of cells, simpleness and convenience for preparation and low cost and are suitable for industrial production; meanwhile, medical resources of the sophocarpine are abundant.
US20130109724 N-aminopyrrolylmethyltetrahydropyridines as anti-cancer agents The compounds herein disclosed are N-aminopyrrolylmethyltetrahydropyridine analogs that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of N-aminopyrrolylmethyltetrahydropyridines have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC50 values against the breast cancer cells that are 6-10-fold less than the IC50 of tamoxifen.
US7947676 Pyrazolo[3,4-d]pyrimidine compounds as antitumor agents The invention concerns compounds of the formula (I) wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man.
US20110064675 Elemental iron nanoparticles Synthesis of iron nanoparticles with a substantially unoxidized iron core and a biocompatible coating is described. The nanoparticles are formed by reacting an iron salt solution with a reducing agent in a substantially oxygen-free environment and exposing the formed iron particles to a biocompatible coating agent in a substantially oxygen-free environment to form coated iron particles. An average diameter of the coated iron particles is between 5 nm and 25 nm. The biocompatible coating can functionalized with cell-specific agents for use as diagnostic and therapeutic agents.
CN103156827A Application of stilbene compounds in treating and preventing AIDS The invention provides an application of stilbene compounds in treating and preventing AIDS. The stilbene compounds have a structural formula represented by the general formula (I), wherein R1, R2, R3, R4, R5 or R6 independently represents hydrogen, hydroxyl, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 acyloxy, halogen, nitro, trifluoromethyl, or cyano, provided that at least one of R1, R2 and R3 is hydroxyl and at least one of R4, R5 and R6 is hydroxyl. In the compounds represented by the general formula (I), the inhibition activity IC50 of a stilbene compound piceatannol against HIV-1 protease reaches 59mum.
US20100016410 Methods and Compositions Related to Eosinophil Regulation Disclosed are compositions and methods for regulating eosinophils.
CN102846616A Aripiprazole preparation and preparation method thereof The invention discloses an aripiprazole preparation which comprises aripiprazole and/or its pharmaceutically acceptable salts, and an auxiliary material, wherein the auxiliary material comprises an anti-oxidant. The anti-oxidant is preferably selected from one or more than one of sodium pyrosulfite, sodium bisulfite, sodium sulfite, thiourea, sodium hyposulfite, L-cysteine, sodium ascorbate, citric acid, sodium citrate, tartaric acid, sodium tartrate, malic acid, butylated hydroxyanisole, butylated hydroxytoluene, ascorbyl palmitate, and propyl gallate; the content of the anti-oxidant is 0.1-10% of the mass of the aripiprazole and/or its pharmaceutically acceptable salts. The invention also discloses a preparation method of the aripiprazole preparation. The aripiprazole preparation of the invention has significantly reduced amounts of related materials, good dissolution property and stability, high bioavailability, and less individual difference. The preparation method of the invention is simple in operation, and low in cost, requires no special equipment, and is easily applicable to industrial production.
EP1309349B1 Pharmaceutical composition and method for the treatment of retroviral infections The invention provides the use of a pyrano[2,3-d:6,5-d'] dipyrimidine derivative for the manufacture of a medicine for the treatment of a retroviral infection in a mammal. It also provides a product containing: (a) one or more derivatives of a pyrano[2,3-d:6,5-d'] dipyrimidine; and (b) one or more anti-retroviral drugs, including drugs effective against one or more retroviral or cellular proteins involved in the entry and/or replication of a retrovirus, in respective proportions such as to provide a synergistic effect against a retroviral infection in a mammal, as a combined preparation for simultaneous, separate or sequential use in retroviral infection therapy.
US20110237539 Spinning Solution and Method for Manufacturing Biomaterial Fibers Disclosed herein are spinning solutions and methods for manufacturing a biomaterial fiber. The spinning solution includes a biologically absorbable material having a haemostatic function, a polysaccharide selected from the group consisting of hyaluronic acid (HA) and gelatin, and a solvent, wherein the polysaccharide and the haemostatic material exist in a weight ratio between about 0.1 to about 3. The method includes steps of wet spinning the spinning solution into the biomaterial fiber.
WO2007071071A1 Oligonucleotides and antiviral uses thereof Mutagenic oligonucleotides and methods for use in anti-retroviral therapeutics are provided. The oligonucleotides described herein specifically bind to a target retroviral nucleic acid in a sequence specific manner. This binding stimulates mutagenesis within or adjacent to a target retroviral nucleic acid region. The mutation thus introduced inactivates completely or partially the function of the gene encoded by the nucleic acid containing the target site, thereby inhibiting or preventing the replication of the virus.
US20080125397 2 (SULFONYL)ETHYL N,N,N',N' tetrakis(2 chloroethyl)phosphorodia 2-({2-Oxo-2-[(pyridin-3-ylmethyl)amino]ethyl}sulfonyl)ethyl N,N,N′,N′-tetrakis(2-chloroethyl)phosphorodiamidate and its acid addition salts, especially in solid form, their preparation and intermediates in their preparation, formulations containing them, and methods of treatment using them. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
CN101406475A Use of lapatinib for reversing multi-drug resistance of tumor The invention relates to the multi-drug resistance (MDR) of Lapatinib (formula 1) in reversing tumour cells which are mediated by membrane transport proteins (ABC) families such as P-glycoprotein (P-gp), multi-drug resistance related protein (MRP1), breast cancer multi-drug resistance related proteins (ABCG2 and BCRP) and the like. The Lapatinib is used together with anti-cancer drugs such as anthracyclines, catharanthines, taxols, podophyllotoxins, camptothecins and the like to restore the sensitivity of MDR tumor cells to the anticancer drugs. The Lapatinib is applied to combination chemotherapy of drug-resistant patients in clinical chemotherapy or the prevention of drug-resistance generation for the tumor cells.
WO2005082390A1 Fat accumulation inhibitors [PROBLEMS] To provide fat accumulation inhibitors which originate from natural products and exhibit an effect of inhibiting fat accumulation per body weight without harmful effects on the human body. [MEANS FOR SOLVING PROBLEMS] The invention relates to fat accumulation inhibitors containing as the active ingredient fruit polyphenols originating from plants such as rosaceous plants, particularly from ripe or unripe apple fruit, specifically proanthocyanidins such as procyanidins; and to foods, drinks, food additives, drugs, quasi drugs and feeds, containing the same.
WO2011057974A1 Propane-i-sulfonic acid {3-[5-(4-chloro-phenyl)-1h-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide compositions and uses thereof The present invention is related to an improved method for the manufacture of Micro- precipitated Bulk Powder (MBP) containing the active pharmaceutical ingredient Propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide and Hydroxypropylmethylcellulose Acetate Succinate (HPMCAS). The invention is further directed to pharmaceutical compositions containing said MBP, as well as its use in the manufacture of medicaments for the treatment of cancer. Formula (I).
US20090227976 Multiple biocompatible polymeric strand aneurysm embolization system and method Some embodiments includes a system that includes a catheter including a distal portion for location at least partially in an aneurysm, the catheter including a proximal portion, the catheter to transport a biocompatible polymeric strand to an aneurysm, a biocompatible polymeric strand sized to slide through the catheter and a heated excise collar coupled to the distal portion of the catheter, the heated excise collar to provide radial heat from the catheter inward to melt and excise the biocompatible polymeric strand.
US20120245108 Method of modulating complement factor b (cfb) expression in cells The present invention relates to a method of modulating complement factor B (CFB) expression in cells, comprising administering an effective amount of tannic acid to the cells. This method can be applied in treating or prophylaxis of the disease, disorder or medical condition associated to complement factor B (CFB) expression.
US7588782 Rare earth metal compositions for treating hyperphosphatemia and related methods Rare earth metal compounds, particularly lanthanum, cerium, and yttrium, are formed as porous particles and are effective in binding metals, metal ions, and phosphate. A method of making the particles and a method of using the particles is disclosed. The particles may be used in the gastrointestinal tract or the bloodstream to remove phosphate or to treat hyperphosphatemia in mammals. The particles may also be used to remove metals from fluids such as water.
CN1944383A Alpha-alkoxy propionic acid compounds and their preparing method and medicine use The present invention discloses alpha-alkoxy propionic acid compounds as shown and their stereoisomer, optical isomer, raceme, physiologically acceptable salt, solvolyte and crystal form, the preparation process of the compounds, medicine preparation of the compounds, and the clinical application of the compounds in treating diseases relevant to insulin resistance.
EP2552200A1 Dimethyl sulfoxide (dmso) formulations for treating autism Embodiments of the invention relate generally to formulations comprising dimethyl sulfoxide (DMSO) to treat behavioral disorders, communication delays, and developmental delays. Several formulations disclosed herein are useful for treating broad autism phenotype disorders, including autism spectrum disorders (e.g., autism).
WO2012052372A1 Tetrahydroquinoline derivatives used as ampk activators A compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein R1 to R7 have the significance given in claim 1, can be used as a medicament.
CN1939271A Oral preparation containing erythrocin and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains erythro mycin. Its preparing process is also disclosed.
CN101683356A Water-soluble vitamin preparation for injection and preparation method thereof The invention relates to a water-soluble vitamin preparation for injection and a preparation method thereof. The water-soluble vitamin preparation for injection is used for supplying human bodies withvarious water-soluble vitamins for physiological needs every day, so that various related biochemical reactions in the organisms can be carried out normally. The composition can be made into a freeze-dried preparation by directly or indirectly adding pharmaceutically acceptable forming agents and the like through conventional techniques. The composition has the characteristics of favorable dissolubility, stable quality, high safety and effectiveness, and the like.
CN103565818A Applications of nicotinamide adenine dinucleotide (NAD<+>) in preparation of medicine used for curing liver damages caused by chemotherapy drug doxorubicin hydrochloride The invention relates to applications of nicotinamide adenine dinucleotide in the field of pharmacy, and more specifically relates to applications of nicotinamide adenine dinucleotide in preparation of a medicine used for curing liver damages caused by chemotherapy drug doxorubicin hydrochloride. NAD<+> is capable of preventing and treating liver damages caused by chemotherapy drug doxorubicin hydrochloride effectively; and it is also found that NAD<+> is capable of killing glioma cells, neuronal tumor cells, gastric cancer cells, renal tumor cells or breast tumor cells effectively, but possesses no killing effect on normal primary cells.
WO2009009739A2 Methods and compositions for facilitating cell death of cancer stem cells and for treating cancer The invention provides methods and compositions for reducing the number of cancer stem cells in a mixed population of differentiated cells (for example, cancer cells) and cancer stem cells. The cancer stem cells, if present, can be more resistant to traditional drug-based therapies and can provide a source for new, differentiated cancer cells associated with the development of drug-resistance and more aggressive phenotypes. When combined with traditional cancer therapies, for example, drug-based therapies, the methods and compositions of the invention provide a more effective way for treating cancer and can provide a model system for developing new cancer therapies and new treatment modalities.
EP1501517A1 Pharmaceutical combination for the treatment of benign prostatic hyperplasia or for the long-term prevention of acute urinary retention The present invention relates to a new pharmaceutical combination for treating benign prostatic hyperplasia (BPH) or for the long-term prevention of acute urinary retention (AUR).
EP1525001A1 Conjugates of porphyrin compounds with chemotherapeutic agents Conjugates of porphyrins with chemotherapeutic agents are disclosed, as well as methods of making the conjugates and methods of treating patients with the conjugates. Porphyrin compounds, such as mesoporphyrin IX, can be covalently linked to chemotherapeutic compounds, such as doxorubicin. The resulting conjugates display decreased systemic toxicity, while preserving the antineoplastic effects of the chemotherapeutic agent. The conjugates are thus useful in treating cancer and other diseases marked by uncontrolled cell proliferation.
EP2556079A2 Polyol modified aminoglycoside-lipid conjugates In some aspects, the present invention provides aminoglycoside derivatives thereof that exhibit antibacterial activity. In some aspects, the aminoglycoside derivatives comprise compounds consisting of (a) an ammoglycoside group and (b) at least one hydrophobic carbamate and alkoxy group to the primary or secondary hydroxy position of the aminolvcoside group and salts thereof. Additionally, methods of treating and preventing bacterial infections using the aminoglycoside derivatives are also provided
CN101585809A Novel compound with antibacterial and antitumor activities The invention provides a novel compound with antibacterial and antitumor activities, discloses a novel lactam compound and a preparation method and application thereof, in particular relates to a novel lactam compound prepared by microbial fermentation and application thereof, and belongs to the field of biotechnology. The chemical name of the lactam compound is (6S, 8aS, 9S, 11S, 12aR)-6-hydroxy -9,10-dimethyldecahydrobenzo[d]aza-decm-pentaene-2,4,12(3H)-triketone. The novel lactam compound has the advantages that experiments show that the compound has obvious inhibiting effect on the growth of fusarium oxysopoyum f.sp.cubence race 4 (FOC4), human hepatocarcinoma cell SMMC-7721 and mouse sarcoma cell s180, and has lower toxicity; therefore, the compound can be used as a raw material of anti-fungal pesticide or an anticancer medicament and has better application prospect; moreover, the preparation method for the compound is a biofermentation method, has simple steps and lower cost and is propitious to industrialized popularization and implementation.
US7384963 2′-Methyl-5-(1,3,4-oxadiazol-2-yl)1, 1′-biphenyl-4-carboxaide derivatives and their use as p38 kinase Compounds of formula (I), wherein R1 is a phenyl group which may be optionally substituted; R2 is selected from hydrogen, C1-6 alkyl and (CH2)p—C3-7cycloalkyl; R3 is the group: (Formula II), R4 is selected from hydrogen and C1-4 alkyl; U is selected from methyl and halogen; X and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4, and may be optionally substituted with up to two groups selected independently from C1-6 alkyl; n is selected from 0, 1 and 2; p is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors
WO2010035253A1 Effective nitric oxide generating preparations The invention discloses an orally compatible, palatable composition suitable as a Nitric Oxide (NO) in vivo enhancer. The aforementioned composition comprises an effective dosage of a soluble nitrate substrate. The main innovation is that the nitrate substrate is adapted for prolonged interaction with the saliva of the patient. Furthermore the nitrate substrate is suitable for at least partial nitrification to endothelially absorbable nitrite ions by the naturally occurring anaerobic nitrifying bacteria of the saliva.
US20060062842 Method of administering a compound to multi-drug resistant cells A composition for administration of a therapeutic compound to a multi-drug resistant cell in a person suffering from a drug-resistant cancer is described. The composition is composed of a carrier molecule and a folate targeting ligand, which is covalently attached to the carrier, and the therapeutic compound. In one preferred embodiment, the carrier is a liposome having a surface coating of hydrophilic polymer chains where a folate ligand is attached to the free distal end of at least a portion of the hydrophilic polymer chains, and the therapeutic agent is entrapped in the liposomes. The composition is effective to achieve accumulation of the therapeutic compound in the cell in an amount sufficient to be cytotoxic. Also described are methods for administering a therapeutic compound to a person suffering from a multi-drug resistant condition.
CN103656304A Detoxification and detumescence poultice for venomous snake bites and preparation method of poultice The invention discloses a detoxification and detumescence poultice for venomous snake bites and a preparation method of the poultice. The poultice comprises raw materials in parts by weight as follows: 18-24 parts of amur cork tree barks, 12-16 parts of spreading hedyotis, 10-15 parts of Chinese lobelia, 10-15 parts of radix angelicae, 8-14 parts of wild chrysanthemum, 6-12 parts of root barks of peony tree, 10-15 parts of trogopterus dung, 5-10 parts of ligusticum wallichii, 14-18 parts of mint, 16-22 parts of roots of mysorethorn, 10-15 parts of selfheal, 15-20 parts of fructus forsythiae, 10-15 parts of ramie roots, 5-10 parts of Japanese thistle herb, 10-15 parts of rhizoma acori tatarinowii, 5-10 parts of Chinese tallow leaves, 10-15 parts of Chinese teasel roots, 5-10 parts of Japanese violet herb or roots, 12-18 parts of lalang grass rhizome, 10-15 parts of copperleaf herb, 10-15 parts of musk, 5-10 parts of mirabilite, 8-12 parts of camphor and 10-15 parts of tobacco tar. The poultice has effects of clearing heat, detoxification, cooling blood, detumescence, activating blood, removing blood stasis, relieving pain, resisting inflammation, stopping bleeding and promoting granulation, can be used for treating various venomous snake bites, and is exact in efficacy, remarkable in curative effect, quick in effect, short in treatment course, capable of removing vivotoxin rapidly and completely and convenient to use; and the cure rate reaches 100%.
EP1531799A1 Nanoparticulate formulations comprising hmg coa reductase inhibitor derivatives ("statins"), novel combinations thereof as well as manufacturing of these pharmaceutical compositions The present invention is directed to nanoparticulate compositions comprising statin such as lovastatin or simvastatin including surface stabilizer. The statin particles of the composition have an effective average particle size of less than about 2000 nm. In another aspect of this invention, novel combinations of statins and other cholesterol lowering agents are described and methods of using same are taught.
US20110118301 Amino-Aza-Adamantane Derivatives and Methods of Use The invention relates to amine-substituted aza-adamantane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. Radiolabelled compounds useful for evaluating the binding affinity to α7 nicotinic acetylcholine receptors also are described.
WO2009090222A1 Naphthyridin-2(1h) -one compounds useful as antibacterials Compounds of Formula (I), wherein substituents R1, R2 and R5 are as defined, and Ar represents substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, furanyl, imidazolyl and thiophenyl; compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
US20100297242 Ldl-like cationic nanoparticles for deliverying nucleic acid gene, method for preparing thereof and method for deliverying nucleic acid gene using the same Disclosed are a LDL-like cationic nanoparticle for delivering a nucleic acid gene with improved transfection efficiency and stability, which is surface modified and re-constructed by mimicking lipid components of a natural LDL, a method for preparation of the same, and a method for delivering nucleic acid genes using the same. The cationic nanoparticle of the present invention could effectively be applied in treatment of cancer that overexpress LDL receptors.
CN102861206A Sterilizing and disinfecting aerosol for skin mucous membrane and preparation method thereof The invention relates to a sterilizing and disinfecting aerosol for skin mucous membrane and a preparation method of the sterilizing and disinfecting aerosol for the skin mucous membrane. The sterilizing and disinfecting aerosol for the skin mucous membrane is strong in sterilizing effect, good in disinfecting effect, non-irritating to the skin mucous membrane, safe and reliable, and particle and convenient, thereby being suitable for the use of skin, hands and feet, nasal cavities, oral cavities and vaginas of the human body.
EP1699465B1 The use of hydrocortisone to treat depression We describe a treatment regime for the treatment of conditions which result from the abnormal secretion of cortisol.
US20120189543 Compositions and Methods for Detecting and Treating Implant Loosening and Osteolysis Methods and compositions for detecting, diagnosing, and treating osteolysis and implant loosening are disclosed.
WO2013054338A1 2-thio-imidazole derivatives as tgr5 modulators The present invention relates to compounds of the general Formula I their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, their N-oxide, metabolites, polymorphs, use of these compounds in medicine for treating diabetes (TGR5 modulators) and the intermediates involved in their preparation.
CN101445566B Arginine amino polysaccharide containing NO increasing and releasing agent and production method thereof The invention discloses arginine glucidamin containing in an NO increasing and releasing agent and a production method thereof, which comprises the step of the preparation of glucidamin, arginine ascorbate, and arginine glucidamin containing in the NO increasing and releasing agent and the like by using the enzyme method. The invention has the advantages of simple process, easily obtained raw material and low production cost. The product is a novel NO increasing and releasing agent which is a super compound formed by coordinating the arginine and the glucidamin under the action of ascorbic acid and is an excelled intrinsic carrier oxygen transferring body, and can be used as preferred raw material and food additives of health care medicaments for treating the absence of intrinsic nitrogenoxide.
CN1957913A Composition of anti cancer medication prepared from carried platinum category compound and consubstantial hydrolytic agent A slowly-release anticancer medicine in the form of injection or implant is disclosed. Said slowly-release injection is composed of a special solvent containing suspending aid and the slowly-release microballs consisting Pt compound, iterstitial hydrolyte and slowly-releasing auxiliary. Said Pt compound is chosen from cisplatin, carboplatin, etc. Said interstitial hydrolyte is chosen from collagenase, relaxin, etc. Said slowly-releasing auxiliary is chosen from polylactic acid, polyethanediol, etc.
EP2079691A1 Substituted indeno[1,2-b]indole derivatives as novel inhibitors of protein kinase ck2 and their use as tumour therapeutic agents, cytostatics and diagnostic aids Synthesis of novel substituted indeno[1,2-b]indole derivatives of the type of 5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-diones and 5H-indeno[1,2-b]indole-6,9,10-triones, which show pronounced inhibition of the human protein kinase CK2, and the use thereof as active ingredients in medicaments and/or drug products in particular for the treatment of neoplastic diseases.
US7544700 4-chloro-N-((5-((4-(hexylamino)piperidin-1-yl)sulfonyl)thien-2 -yl)methyl)benzamide for example; JUN kinase inhibitors to treat nervous system disorders, cancer, cardiovascular and autoimmune disorders The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl which is substituted with at least one ionizable moiety to which a lipophilic chain is attached and which is containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.
US20120022030 Tetracyclic Lactame Derivatives The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.
CN1895270A Anoxia and fatigue-resisting health-care oxygen, its preparation and use as health-care product A health-care oxygen product in the form of beverage, toothpaste mate, or medicine for treating constipation is proportionally prepared from sodium (or potassium) chlorite, sodium (or potassium) bicarbonate, sodium (or potassium) carbonate, and deionized water through preparing the aqueous solution of sodium (or potassium) bicarbonate and sodium (or potassium) carbonate, dissolving the sodium (or potassium) chlorite in it, and dripping it in purified water, cold boiled water, mineral water, or sugar solution. It can improve immunity, relieving fatigue, and treating anoxia.
WO2010150865A1 Crystals Provided are the following novel crystals of 2-{4-[N-(5,6-diphenylpyradin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (hereinafter, referred to as "compound A"): I-form crystals of the compound A which give an X-ray powder diffraction spectrum having diffraction peaks at least at diffraction angles (2θ) of 9.4º, 9.8º, 17.2º, and 19.4º; II-form crystals of the compound A which give an X-ray powder diffraction spectrum having diffraction peaks at least at diffraction angles (2θ) of 9.0º, 12.9º, 20.7º, and 22.6º; and III-form crystals of the compound A which give an X-ray powder diffraction spectrum having diffraction peaks at least at diffraction angles (2θ) of 9.3º, 9.7º, 16.8º, 20.6º, and 23.5º.
US20100104583 Gene Polymorphisms in VEGF and VEGF Receptor 2 as Markers for Cancer Therapy The invention provides compositions and methods for determining the likelihood of successful treatment with anti-angiogenic antibodies or equivalent thereof, in combination with a pyrimidine based antimetabolite and a platinum-based alkylating agent based therapy. The methods comprise determining the genomic polymorphism present in a predetermined region of a gene of interest and correlating the polymorphism to the predictive response. Patients identified as responsive are then treated with the appropriate therapy.
WO2013000280A1 9-sulfonyl-9h-purine derivative, preparation method and use thereof Disclosed are a 9-sulfonyl-9H-purine derivative as represented by Formula (I), a preparation method and use thereof. The compound represented by Formula (I) is provided with anti-chronic hepatitis C virus activity. [Formula I]
US20120282259 Mutant smoothened and methods of using the same The emergence of mutations in tyrosine kinases following treatment of cancer patients with molecular-targeted therapy represents a major mechanism of acquired drug resistance. Here, we describe a mutation in the serpentine receptor, Smoothened (SMO), which results in resistance to a Hedgehog (Hh) pathway inhibitor in medulloblastoma. A single amino acid substitution in a conserved aspartic acid residue of SMO maintains Hh signaling, but results in the inability of the Hh pathway inhibitor, GDC-0449, to bind SMO and suppress the pathway. This mutation was not only acquired in a GDC-0449-resistant mouse model of medulloblastoma, but was identified in a Medulloblastoma patient following relapse on GDC-0449. The invention provides screening methods to detect SMO mutations and methods to screen for drugs that specifically modulate mutant SMO exhibiting drug resistance.
US20070244123 Heterocycle-carboxamide derivatives as raf kinase inhibitors Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine or cardiac hypertrophy.
US20100234286 Preterm formula The present invention relates to a method and a composition for feeding low birthweight infants (LBW infants), very low birthweight infants (VLBW infants), extremely low birthweight infants (ELBW infants) and preterm infants for improving oral tolerance.
CN101862340A Application of lactose derivatives Gu-4 used as medicine for treating endotoxin shock The invention relates to application of lactose derivatives Gu-4 used as inhibitors of integrin CD11b for effectively treating endotoxin shock. Through experiments, the lactose derivatives Gu-4 can effectively prolong the survival time of endotoxin shock mice and obviously improve the survival rate.
WO2008149838A1 Novel fractionation product of royal jelly, method for production of the same, and use of the same Disclosed are: a fractionation product of royal jelly, which still retains a useful physiological activity of royal jelly and has little concerns that an allergic condition may be induced; a method for producing the fractionation product; and use of the fractionation product in various compositions including a food/beverage, an animal feed, a fish bait, a pet food and an external preparation for the skin such as a cosmetic product each containing the fractionation product. Specifically disclosed are: a fractionation product of royal jelly, which comprises 1 part by mass of 10-hydroxy-2-decenoic acid and less than 0.05 part by mass of a protein derived from royal jelly, which has a useful physiological activity of royal jelly, and which has such a property that no allergenicity against the fractionation product is detected by the passive cutaneous anaphylaxis on a rat using a serum from a mouse immunized with such an amount of the fractionation product that 45 μg of 10-hydroxy-2-decenoic acid is contained in the fractionation product; a method for producing the fractionation product; and use of the fractionation product.
USRE40839 Taxol treatment of cancer The present invention is a method of treatment for a patient with cancer. In particular, it is a method of treating patients having lymphomas and breast cancer using the microtubule agent, Taxol. The present method of administration, serves to prevent or retard the adverse side effects associated with Taxol and reduces the chances of a patient developing mdr Taxol resistance. The novel method of treatment provides a low-dose, long-term exposure to Taxol in a patient.
CN101040883B Andrographis root extraction and its preparing process and application in preparing antithrombotic medicine The invention provides a creat root extractive, characterized in that it comprises 53.28-68.53% chromocor with 6.85-11.38% 5, 2'-dihydroxy-7, 8-dimethyl ketone). And the preparation comprises that immerging creat root powder into alcohol, heating at normal pressure, refluxing and extracting, passing the alcohol extractive through large-hole adsorption resin, washing with alcohol, collecting the washed liquid whose alcohol density is 60-90%, depressurizing and concentrating, atomizing and drying, while the preparation holds the flavonoids as 7-O-methyl wogonin, creat chromocor, 5-hydroxy-7, 8,2' 3'-tetrahydroxyflavone, 5-hydroxy-3, 7, 8, 2'-tetrahydroxyflavone, 5, 2'-dihydroxy-7, 8-dimethylketone, to hole the natural characters of creat root.
EP2687204A1 Vector for pulmonary delivery, inducing agent, and uses The present invention provides a liposome having excellent lung migration ability that had not existed hitherto, by including GALA or Chol-GALA in the liposome. Furthermore, by using the liposome, a pulmonary delivery carrier having a stronger knockdown effect of siRNA when compared to existing carriers is provided.
US7109195 Hexacyclic compounds and their therapeutic use The present invention relates to hexacyclic compound of the formula [1], wherein Z, R3 and R4 are as identified therein, and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of cell proliferative disorders.
CN102603575A Rhein-arginine eutectic compound, and preparation method, purification method and application thereof in preparation of medicines for treating diabetic complications The invention relates to a rhein-arginine eutectic compound, and a preparation method, a purification method and application thereof in preparation of medicines for treating diabetic complications. The rhein-arginine eutectic compound is an eutectic substance formed by rhein and L-arginine, the mol ratio of the active medicine component of the rhein to the L-arginine is 1:1, and the X-ray diffractogram of the eutectic powder has the characteristic peaks of 9.22 degrees, 10.34 degrees, 12.28 degrees, 26.05 degrees, 26.58 degrees and 27.57 degrees 2theta. The medicines for treating diabetic complications are medicines for treating diabetic cardiopathy, medicines for treating diabetic macroangiopathy, medicines for treating diabetic nephropathy, medicines for treating diabetic orchiopathy, medicines for treating complicated male sexual dysfunction of diabetes, or medicines for treating diabetic impotence. The invention can increase the solubility and dissolution of the medicines, enhance the purity and stability of the rhein-arginine eutectic compound, reduce the impurity content and hygroscopicity, enhance the bioavailability and improve the release characteristic.
CN1904059A Production method of konjak mannose using cellulase The present invention relates to a production method for preparing konjak mannoligose by using cellulase. Its technological process includes the following several procedures: enzymolysis, filtraction, decoloring, concentration and drying. It is characterized by that said invention adopts non-specific commercial enzyme (including cellulose and hemicellulase), and utilizes centrifugal filtering and membrane filtering combined process, so that said invention can obtain high-purity konjak mannoligose. Besides, said invention also provides the concrete requirements and steps of the above-mentioned every procedure.
WO2009069012A1 Process and intermediates for the preparation of substituted 1, 3-oxathiolanes, especially lamivudine The present invention relates to process and intermediates for the preparation of substituted 1,3-oxathiolanes. The present invention specifically relates to a process for the preparation of lamivudine.
WO2008102017A3 Food comprising polyunsaturated fatty acids for the prevention of chronic diseases The present invention is related to a method for the prevention and possibly the treatment of chronic diseases, preferably inflammatory associated chronic diseases that may affect an animal including a human, by the administration of a sufficient amount of a (functional) food or feed to the diet of this animal.
WO2008096200A2 Purifier device for burnt gases from internal combustion engines A purifier device for burnt gases discharged from internal combustion engines comprising a sealed compartment or recipient container (1) which has an inlet port (4) for gases coming from the exhaust pipe (2), and an outlet port (5) at the end of the purified gases outlet pipe (3). In addition, the device has a water-repellent membrane (10) above the level (8) of the solvent (9), with the purpose of enabling the gas to exit towards a chamber (11) and also containing the solvent (9) so that it does not leak from the device via the outlet port (5). Fitted in the inlet port (4) is a lip-type retention valve (6), which in the open position allows for free flow with positive differential pressure and in the base (18) of the device is a purging port (13) which connects with a conventional recirculation, cooling and filtering circuit for the solvent element (9). The cover (17) of the purifier has a return port (14) for the recirculation system, which is not communicated with the chamber (11) and which includes another lip valve (19). The fitting of an aspirating means for gases, such as a turbine (12) in the gas intake pipe of the device (2) is to facilitate the opening of the retention valve (6).
WO2012032209A3 Pharmaceutical composition for the treatment of dry eye The invention relates to therapeutic compositions for the treatment of dry eye and, more specifically, compositions comprising a TRPM8 receptor agonist ligand. In addition, the invention relates to therapeutic compositions for the treatment of epiphora and, more specifically, compositions comprising a TRPM8 receptor antagonist.
EP1492821B1 Iron dextrin compounds for the treatment of iron deficiency anaemia An iron-dextrin compound for treatment of iron deficiency anaemia comprising hydrogenated dextrin having a weight average molecular weight equal to or less than 3,000 Dalton and a number average molecular weight equal to or higher than 400 Daltons, in stable association with ferric oxyhydroxide. As the molecular weight of the dextrin must be narrow it is another important feature of the invention that the 10 % fraction of the dextrins having the highest molecular weight has an average molecular weight of less than 4500 Daltons, and that 90 % of the dextrins are having molecular weights of less than 3000 Daltons. It is further important that the 10 % fraction having the lowest molecular weight has a weight average molecular weight of 340 Daltons or more.
US8338403 Drug for improving hyperglycemia A compound having a hyperglycemia improving effect and a hemoglobin A1c lowering action such as 4-methylcholest-7-en-3-ol, 4-methylergost-7-en-3-ol and 4-methylstigmast-7-en-3-ol is used as an active ingredient of a drug or food or drink for improving hyperglycemia.
US20080199550 Novel Anticancer Agent, Methods for Obtaining the Same and Pharmaceutical Compositions Thereof Disclosed herein a herbal anticancer agent comprising the extract of plant Sphaeranthus indicus or group of compounds obtained from the plant Sphaeranthus indicus. The present invention also discloses a pharmaceutical composition comprising the said agent, methods for preparing the composition and methods of treating all kinds of cancer in mammals including human beings. The methods of making the plant extract, methods for obtaining the active constituents are also dealt with.
US20090306209 Enteric-coated formulations of polyethylene glycol and one or more soluble amino acids for oral ingestion and enhanced uptake of same Oral amino acid formulations comprising polyethylene glycol are enteric coated. Most preferred amino acids are leucine, glutamine, and arginine. The most preferred polyethylene glycols have an average molecular weight of from 3150 to 3685, although for particular formulation formulations and particular uses, the average molecular weight polyethylene glycols may range from 190 to 9000.
CN102764235A Strontium ranelate dry suspension and preparation method thereof The invention discloses a strontium ranelate dry suspension which is a drug for treating osteoporosis and a preparation method of the strontium ranelate dry suspension. The dry suspension is composed of strontium ranelate particles and additionally-added auxiliary materials, wherein the strontium ranelate particles are formed by strontium ranelate or powder of hydrate of the strontium ranelate through a dry granulating method, and the medium diameter of the strontium ranelate particles ranges from 170 to 480 um. The preparation provided by the invention has good stability and mobility of particles, and can better meet the requirements of granulation machines for split charging during commercial production.
WO2009043582A1 Nicotinamide n-oxide derivatives as vanilloid-1 receptor modulators Vanilloid receptor modulators of formula (I) wherein X is selected from phenyl, naphthyl, pyridine, quinoline or isoquinoline and Y is an optionally substituted phenyl or pyridyl ring, and related processes for the preparation and pharmaceutical uses for treatment of inflammatory conditions.
US20120315319 Guided bone regeneration membrane and manufacturing method thereof A guided bone regeneration material is disclosed. The guided bone regeneration material includes biodegradable fibers produced by an electro spinning method. The biodegradable fibers produced by the method include a silicon-releasing calcium carbonate and a biodegradable polymer. The silicon-releasing calcium carbonate is a composite of siloxane and calcium carbonate of vaterite phase. The biodegradable fibers may be coated with apatite. When the guided bone regeneration material is immersed in a neutral aqueous solution, silicon species ions are eluted from the calcium carbonate. The guided bone regeneration material excels in bone reconstruction ability.
EP2739280A1 A method of managing chemotherapy induced alopecia or cachexia or both The present disclosure is related to management of chemotherapy induced side effects namely cachexia and alopecia by administering a pharmaceutical composition comprising pentameric type A procyanidin flavonoid, trimeric procyanidin flavonoid and tetrameric procyanidin flavonoid, optionally along with pharmaceutical excipients.
CN102008722A Compound preparation of naproxen and triptan drugs for treating migraine The invention discloses a compound preparation of naproxen and triptan drugs for treating migraine, comprising main compositions and a matched pharmaceutically acceptable vector, wherein the main compositions include the following components in weight ratio: 250-1000mg of the naproxen or a pharmaceutically acceptable salt thereof and 1.0-80mg of the triptan drugs or a pharmaceutically acceptable salt thereof. The invention reduces the adverse reaction relative to the increase of a certain dosage and can efficiently treat the migraine according to the drug complementary synergism fully exerted by drug combination and has the advantages of short treatment course, fast effect, little side effect and low cost.
US20050209243 7-[2-[4-(2-methoxyphenyl)piperazinyl]-ethyl]-1,3-dimethylxanthine (KMUP-1); muscle relaxants, endothelium-dependent NO releasing, learning and memory activities, erectile dysfunction The present invention provides the pharmaceutical compositions for relaxing corpus the cavernosal smooth muscle, increasing the intracarvernosal pressure, and enhancing learning and memory activities.
WO2012158979A1 Quinazoline-7-ether compounds and methods of use The invention provides quinazoline-7-ether derivatives, particularly 4-anilinyl-6- butenamido-quinazoline-7-ether derivatives that are inhibitors of the receptor protein tyrosine kinases (RTK). The compounds are useful in the treatment of diseases and disorders where RTK activity is implicated such as a hyperproliferative diseases (e.g., cancer). Also provided are methods of preparation of the quinazoline derivatives and methods of use as therapeutic agents alone or in a drug combination.
US8188056 Utilizing nucleic acid expression constructs that are delivered into a subject and express stable therapeutic proteins in vivo One aspect of the current invention is a method of preventing and/or treating arthritis and/or preventing or treating lameness in a subject. Additionally, subject quality of life and welfare, and body condition scores are improved by utilizing methodology that administers the nucleic acid expression construct encoding a GHRH or functional biological equivalent to a subject through a parenteral route of administration. Following a single dose of nucleic acid expression vector, subjects are healthier and effects are demonstrated long term without additional administration(s) of the expression construct.
CN101880308A New hopane-type triterpene and preparation method and application thereof The invention belongs to the technical filed of medicines, and relates to the preparation of three new hopane-type triterpenes and applications thereof. The new hopane-type triterpene saponins have the following structure shown in the specification. The new hopane-type triterpene compounds have quinone reductase induced activity, and can be used for development and application of anti-tumor drugsand tumor chemoprevention drugs.
USRE39530 Dimethyl-{[2-(2-methylbenzyloxy)cyclohexyl]phenylmethyl}-amine; analgesically active, treatment of pain, local anaesthetic, antiarrhythmic, antiemetic cardiovascular diseases, urinary incontinence, diarrhea, pruritus, alcohol, drug or medicament dependency, inflammations 3-amino-3-arylpropan-1-ol compounds corresponding to the formula I in which R1 to R5, A and X have the meanings according to claim 1, and their preparation and use as medicaments.
CN103271941A Novel application of zinc chloride serving as medicine for curing human brain glioma The invention relates to the novel application of zinc chloride serving as medicine for curing human brain glioma. According to the invention, voltage-gated channel Hv1 is taken as a target spot, and zinc chloride is taken as medicine for curing human brain glioma. The zinc chloride has a certain restraining effect to growth, migration and infiltration of human brain glioma cell with higher malignization degree. Therefore, the zinc chloride provided by the invention is taken as the medicine for curing human brain glioma, and has a wide prospect.
CN101579321A Preparation process for glimepiride tablet The present invention provides a glimepiride tablet which comprises the following components: glimepiride, a filling agent, adhesive and lubricant. The glimepiride tablet is characterized in that the surfactant is added. The glimepiride tablet of the invention has the advantages of few components, readily available accessory, high disintegration speed, uniform dispersion, complete dissolution at a dissolution rate of more than 95 percent, stable quality prevention of dissolution rate decrease during storage and suitability for long-term storage.
CN102643229A N-((4-chloro-3-trifluoromethyl) phenyl)-N'-((2-fluoro-4-(2-formamyl)-4-pyridyloxy) phenyl) urea and application thereof serving as anticancer medicament The invention relates to N-((4-chloro-3-trifluoromethyl) phenyl)-N'-((2-fluoro-4-(2-formamyl)-4-pyridyloxy) phenyl) urea serving as a vascular endothelial growth factor receptor 2 (VEGFR-2) kinase inhibitor and application of the urea in preparation of a medicament for treating VEGFR-2-mediated diseases.
CN101020638A 1'-acetoxy chavicol acetic ester The present invention discloses a supercritical CO2 extraction and silica gel column chromatographic process for extracting, separating and refining 1'-acetoxy chavicol acetic ester with activity of resisting tubercle bacillus infection from dried galangal rhizome as one kind of Zingiberaceae plant.
CN102552314A Preparation method of compound sodium chloride-potassium chloride infusion solution The invention relates to the field of pharmacy and especially relates to a preparation method of a compound sodium chloride-potassium chloride infusion solution. The invention aims at providing a preparation method of an electrolyte supplement and the electrolyte supplement is the compound sodium chloride-potassium chloride infusion solution containing active components of sodium chloride and potassium chloride. Based on a prescribed dose, each 100ml of the compound sodium chloride-potassium chloride infusion solution contains 0.05 to 0.33g of potassium chloride and 0.7 to 1.1g of sodium chloride. The compound sodium chloride-potassium chloride infusion solution is applied by intravenous injection and is suitable for patients having severe hypokalemia or patients unable to take oral medicines. A potassium supplement dose, potassium concentration and a potassium supplement speed of the compound sodium chloride-potassium chloride infusion solution can be set according to clinical conditions, serum potassium concentration and improvement of a potassium deficiency graph of an electrocardiogram.
CN101129397A Medicine for treating man's sterility and method of preparing the same The invention discloses a medicament for treating male infertility and process for preparation, wherein the medicament comprises the following raw materials (by weight portion): arginine 2+-5%g, zinc gluconate 100+-55%mg, selenium citrate 20+-5%mg, vitamin A 5000+-5%mug, vitamin E 100+-5%mg, L-Carnitine 2+-5%g, clomiphene 50+-5%mg, nucleic acid 100+-5%mg. The process for preparing the medicament consists of mixing the raw materials proportionally, charging excipient, mixing and drying to obtain oral administration preparations.
US20080175866 involved in the adaptation of microorganisms to its environment, particularly the identification of genes responsible for the virulence of a pathogenic microorganisms A method for identifying a microorganism having a reduced adaptation to a particular environment comprising the steps of: (1) providing a plurality of microorganisms each of which is independently mutated by the insertional inactivation of a gene with a nucleic acid comprising a unique marker sequence so that each mutant contains a different marker sequence, or clones of the said microorganism; (2) providing individually a stored sample of each mutant produced by step (1) and providing individually stored nucleic acid comprising the unique marker sequence from each individual mutant; (3) introducing a plurality of mutants produced by step (1) into the said particular environment and allowing those microorganisms which are able to do so to grow in the said environment; (4) retrieving microorganisms from the said environment or a selected part thereof and isolating the nucleic acid from the retrieved microorganisms; (5) comparing any marker sequences in the nucleic acid isolated in step (4) to the unique marker sequence of each individual mutant stored as in step (2); and (6) selecting an individual mutant which does not contain any of the marker sequences as isolated in step (4).
US8535655 Biodegradable polymer—bioactive moiety conjugates The invention relates to a biodegradable polymer comprising a plurality of releasable bioactive moieties, the releasable bioactive moieties being pendant from and covalently bonded to the biodegradable polymer backbone, wherein the biodegradable polymer backbone is formed from monomeric units that are each coupled via a biodegradable moiety, and wherein the bioactive moieties are capable of being released at a rate equal to or faster than the rate of biodegradation of the polymer backbone.
WO2013189237A1 Andrographolide analogue and application of andrographolide analogue to treatment Disclosed are a novel andrographolide derivative and analogue as well as a preparation method of the novel andrographolide derivative and analogue and an application to the treatment, the prevention and the relief on human viruses and neoplastic diseases. The present invention also relates to a medicine composition of the compound and an application as antivirus and anticancer disease medicine. Through chemical synthesis and preparation, semi-synthesis multi-series andrographolide analogues can be obtained. The analogues have the following general formula I.
EP1730133A1 Benzothiophene- and thiochromene containing phenethanolamine derivatives for the treatment of respiratory disorders Compounds of formula (I) and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective β2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).
CN102614165A Use of substituted benzoates (besilates) as selective ligands of estrogen acceptor The invention provides a use of substituted benzoate (besilate) compounds with the formula represented by formula I as selective ligands of an estrogen acceptor. In the formula I, R is selected from phenyl or diphenyl substituted alkyl and aryl (Ar), wherein Ar is phenyl or naphthyl substituted by one to two from hydroxyl, alkyl, alkyloxy and alkanoyl; X is C or S=O; and Y is one to two halogen atoms, OH, alkyl or alkyloxy. According to the invention, a method combining a computer simulating medicine design technology and biological activity test is adopted to effectively screen ligands having selective excitation or antagonism effects on the estrogen acceptor, so the compounds can be used for preparing estrogen acceptor mediated relevant disease treatment medicines as medicinal lead compounds.
US20120172342 Biotherapeutics For the Treatment of Infectious Diseases An occlusive dressing made with an elastomeric gel and one or more active agents is described. The elastomeric gel contains a plasticizing oil phase and a block copolymer agent. Methods of preventing, treating, curing or mitigating an infectious disease and methods of making the dressings are also disclosed.
CA2496780C Crystal for oral solid drug and oral solid drug for dysuria treatment containing the same A crystal for oral solid medicament comprised of indoline compound (KMD-3213) which exerts al-adrenaline receptor blocking effect, is useful as a therapeutic agent for dysuria and is represented by the formula: (I) wherein in the powder X-ray diffraction pattern, the compound is characterized by main peaks of 5.5° ~ 0.2°, 6.1° ~ 0. 2°, 9.8° ~ 0. 2°, 11.1° ~ 0.2°, 12.2° ~ 0. 2°, 16.4° ~ 0.2°, 19.7° ~ 0.2° and 20.0° ~ 0.2° as 2.theta. . There is further provided an oral solid medicament for dysuria treatment containing the crystal as an active ingredient. (see formula I)
US20120245121 Methods for improving bone health in infants using long chain polyunsaturated fatty acids Disclosed are methods for improving bone health, strength and formation in an infant who may be susceptible to developing bone health issues from conception through adolescence. The methods include administration of a nutritional formulation including at least one LCPUFA to a woman during pregnancy and optionally during lactation and breastfeeding of an infant.
WO2007137513A1 A TYPE OF NOVEL 2'-α-HYDROXYALKYL TAXEL COMPOUNDS AND THE PREPARATION METHODS THEREOF The present application discloses a type of 2'-α-hydroxyalkyl taxel compounds with following formula (I), the compositions containing the same and uses thereof. These compounds can effectively inhibit the growth of tumor cells, especially can effectively inhibit the growth of tumor cells having multi-drugs resistance (such as MCF-7/ADR), which are better than Paclitaxel (Taxol®) or Docetaxel (Taxotere®).
CN101032514A Method of preparing oxygen supplying solution for improving economy tissue The process of preparing solution for improving oxygen supply of organism tissue belongs to the field of biomedicine technology. The mother liquid is emulsified perfluoro carbon compound in the granularity of 0.1-0.3 microns. The mother liquid is prepared with the materials including perfluoro triethylamine, perfluoro tripropylamine, perfluoro tributylamine, perfluoro decalin, perfluoro adamantane, phospholipid, distilled water, etc, and through compounding, mixing, emulsifying, filtering and packing. The mother liquid is added with dextran, sodium salt, potassium salt, liver growth factor and other supplementary material based on different uses to prepare different types of oxygen supply solution for oral taking, venoclysis, gastrointestinal perfusing or external use. The oxygen supply solution may be used in treating various diseases caused by anoxia.
US7425642 Anti-diabetic activity, improves insulin resistance and control the blood glucose level more safely, simulates activity of peroxisome proliferator-activated receptor; (1-{(2E)-3-[3-(Bromomethyl)phenyl]prop-2-en-1-yl}-1H-pyrrol-2-yl)(4-methyl-phenyl)methanone A heteroaryl derivative of the formula (1): (wherein Ring Z is an optionally substituted heteroaryl, R1 is a carboxyl group or an alkoxycarbonyl group, etc., W1 and W2 are an optionally substituted lower alkylene, Ar1 is an optionally substituted arylene or an optionally substituted heteroarylene, W3 is a single bond, a lower alkylene, a lower alkenylene, etc., W4 is a single bond, —NR10—, etc., Ar2 is an optionally substituted aryl or an optionally substituted heteroaryl), or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
US20130005718 Compositions and methods of treating chronic pain by administering propofol derivatives Compositions and methods for managing or treating chronic pain are provided. More particularly, methods are provided for managing or treating chronic pain by administering to a patient in need thereof an effective amount of propofol or a propofol derivative having limited anesthetic properties. Methods of modulating HCN channel gating are also provided. Pharmaceutically acceptable compositions for, e.g., modulating HCN channel gating are further provided.
CN102516309A Ruthenium complex capable of inhibiting tumor angiogenesis and preparation method and application thereof The invention belongs to the field of chemical drugs, and discloses a ruthenium complex capable of inhibiting tumor angiogenesis and a preparation method and application thereof. The ruthenium complex provided by the invention has a structure shown in a formula I or II. The preparation method comprises the following steps of: dropwise adding a silver nitrate solution to a sodium salt solution, stirring and reacting, then filtering, washing and vacuum drying a precipitate, and thereby obtaining a ligand O-O; taking ruthenium chloride, L, and lithium chloride to be dissolved in N-, N-dimethyl formamide, heating and refluxing under the protection of argon atmosphere to obtain an intermeidate Ru (L2) Cl22 +; allowing the ligand O-O and the Ru (L2) Cl22 + to be dissolved in an ethanol/water mixed solvent, heating and refluxing to obtain the ruthenium complex shown in the formula I; and allowing the Ru (L2) Cl22 +, 8- hydroxyquinoline, and ammonium acetate to be dissolved in ethanol, and heating and refluxing under the protection of argon atmosphere to obtain the ruthenium complex shown in the formula II. The ruthenium complex has the advantages of good stability, uneasiness in hydrolysis, good solubility, low toxicity, and the ability to inhibit tumor angiogenesis, and is easily absorbed by the human body.
CN103610684A Application of saccharides in preparing medicament for treating platelet quantity related diseases The invention discloses an application of saccharides in preparing a medicament for treating platelet quantity related diseases. Saccharides can be one or more of monosaccharides, oxidation-reduction derivatives of the monosaccharides, oligosaccharides, polysaccharides, composite polysaccharides and glycosides. Platelet quantity related diseases comprise primary or secondary thrombocytosis, and primary or secondary thrombocytopenia. Experiments discover that the antibody at an antiplatelet GPIb (glycoprotein Ib) alpha N terminal can induce activation and death of platelets, the platelets can be quickly removed in liver by macrophagocyte, while the saccharides can remarkably inhibit platelet removal caused by the platelet GPIb alpha antibody, and the platelet quantity can be regulated. The application of the saccharides in preparing the medicament for treating platelet quantity related diseases is provided for the first time, and the novel application of the saccharides is expanded.
CN103656658A Drug for treating intestinal disease and preparation method thereof The invention relates to a drug for treating intestinal disease and a preparation method thereof, and belongs to the technical field of medicines. The drug is prepared by the following raw materials in parts by weight: 100-150 parts of erythrocin, 25-35 parts of starch and 5-10 parts of dextrin. According to the present market pharmacy condition, the erythrocin is selected and used as the active substance, and the situation that the erythrocin is an alkaline antibiotic which is easily damaged by the gastric acid to drop the effect and is damaged in the acid transfusion to drop the effect is considered, so that the stability of product preparations is difficult to guarantee; the drug is absorbed by the mouth instead of the stomach, so that the drug is not degraded to drop the effect when encountering the gastric juice; the drug releases the active components when directly achieving the intestines, and acts all the active components in the focus part; the drug has enough dosage and obvious curative effect, and dose not damage the liver and the stomach.
WO2008136331A1 BRANCHED α-GLUCAN, α-GLUCOSYLTRANSFERASE PRODUCING THE SAME, METHOD FOR PRODUCING THE SAME AND USE THEREOF It is intended to provide a glucan useful as a water-soluble dietary fiber, a method for producing the same, and use thereof. The object is achieved by providing a branched α-glucan, which is an α-glucan including glucose as a constituent sugar and is characterized by having the following features based on a methylation analysis: (1) a ratio of 2,3,6-trimethyl-1,4,5-triacetylglucitol to 2,3,4-trimethyl-1,5,6-triacetylglucitol is in the range from 1:0.6 to 1:4; (2) the total amount of 2,3,6-trimethyl-1,4,5-triacetylglucitol and 2,3,4-trimethyl-1,5,6-triacetylglucitol is 60% or more of partially methylated glucitol acetate; (3) the amount of 2,4,6-trimethyl-1,3,5-triacetylglucitol is 0.5% or more and less than 10% of partially methylated glucitol acetate; and (4) the amount of 2,4-dimethyl-1,3,5,6-tetraacetylglucitol is 0.5% or more of partially methylated glucitol acetate, a novel α-glucosyltransferase producing the branched α-glucan, a method for producing the same and use thereof.
EP1496885A1 Use of conjugated linoleic acid derivatives The invention concerns the use of conjugated linoleic acid (=CLA) or derivatives thereof, such as partial glycerides or triglycerides, alkyl esters or salts for the production of a food, a food supplement or a pharmaceutical preparation with the property to prevent or to cure influenza, to boost the effects of an influenza vaccination and / or to alleviate the effects of an influenza vaccination in humans and / or animals.
CN102212021A Sodium paeonol sulfonate crystalline hydrate, and preparation method and application thereof The invention relates to a sodium paeonol sulfonate crystalline hydrate, and a preparation method and application thereof. The crystalline hydrate has high storage stability, and is applicable to the preparation of analgesic and anti-inflammatory drugs for humans and mammals, such as analgesic and anti-inflammatory drugs capable of treating and preventing edema pain after fracture, rheumatism, rheumatoid, prolapse of lumbar intervertebral disk, cervical spondylosis, femoral head necrosis and various wounds and pain and swelling after surgery, and the preparation of drugs capable of treating and preventing coronary heart diseases, angina pectoris, myocardial infarction, arrhythmia, ischemic cerebral diseases, peripheral circulation disorder and other diseases of humans and mammals.
US20090098054 Methods and compositions relating to promoter regulation by muc1 and klf proteins This invention relates to regulation of cell signaling, cell growth, and more particularly to the regulation of cancer or inflammatory cell growth and/or activation. The invention provides methods of, and compositions useful for, inhibiting interactions between MUC1 and a kruppel-like factor (KLF), method of inhibiting interactions between a KLF protein and the p53 promoter, methods of inhibiting the interaction between MUC1 and the p53 promoter, methods of increasing p53 activity, and methods of increasing histone acetylation. The invention also provides screening methods for identifying compounds that inhibit the aforementioned interactions. Pharmaceutical compositions containing the identified compounds can be useful in treating cancers and inflammatory conditions.
US20110184054 Alpha-lipoic acid concentrate A water-free concentrate, consisting of ubiquinone Q10, a medium-chained triglyceride or triglyceride mixture, α-lipoic acid and/or its derivative as well as one or more emulsifiers with HLB value between 9 and 19 permitted according to the foodstuff or drug laws has been described.
WO2013006020A3 Composition comprising pyruvic acids for protecting nerve cells The present invention relates to a composition for protecting nerve cells, and to a functional health food, which comprise pyruvic acids or pharmaceutically acceptable salts thereof so as to inhibit nerve cell apoptosis caused by ethanol. The present invention further relates to a method for protecting nerve cells from the nerve cell apoptosis caused by ethanol, and to a method for treating neurological disorders, which involve injecting the composition into an individual. The composition for protecting nerve cells of the present invention may inhibit apoptosis induced by ethanol, and therefore may be widely used in the prevention and treatment of nerve damage caused by chemicals such as ethanol.
US20080254131 core comprising a water insoluble polymer and acetylcholinesterase inhibitor, a release rate controlling coatings is surrounding the core including a release retarding excipient; administered less frequently, provide more stable blood levels; improve pharmacokinetic; dementia, mania, nicotine dependence Controlled-release galantamine formulations, including controlled-release particles, pellets, granules, and spheres are described. Controlled-release particles, pellets, granules, and spheres with immediate release top-coat are also described. Method of preparing such formulations and method of treating a variety of disorders are also disclosed.
US20100216823 Spirocyclic Derivatives The invention provides compounds of formula (I): wherein m, n, X, R1, A, B, R2 and R3 have the meanings given in the specification, and pharmaceutically acceptable salts, solvates, polymorphs and prodrugs thereof. The compounds are PDE7 inhibitors and have a number of therapeutic applications, particularly in the treatment of pain, especially neuropathic pain.
WO2008052078A2 Benzoxathiine and benzoxathiole derivatives and uses thereof Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R1, R2, R3, R4, y, n, m, p, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
CA2610481A1 3-ester prodrugs of estradiol The present invention is a prodrug derivative of estradiol according to Formula I:
US20070299128 Use of Tryptophan Derivatives for the Specific Cytostatic Treatment of Serotonin-Producing Tumors The invention relates to the use of tryptophane-derivatives for the specific cytostatic treatment of serotonin-producing tumors, such as, for example carcinoids and the like. Areas of application of the invention are in the field of medicine and pharmaceutical industry.
CN103167874A Use of mexiprostil in the treatment of inflammatory bowel disease and/or of irritable bowel syndrome The invention relates to the use of mexiprostil in the treatment and/or prevention of inflammatory bowel disease and of irritable bowel syndrome, to the combinations of mexiprostil with other drugs, and also to a novel method for the synthesis of mexiprostil.
EP2417135A1 Substituted triazolopyridines and analogs thereof The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.
CN103585158A Medicinal composition and its application in preparation of liver cancer treatment medicines The invention discloses a medicinal composition and its application in preparation of liver cancer treatment medicines. The composition is composed of sulforaphen and oleanolic acid, the composition containing sulforaphen and oleanolic acid can substantially inhibit the activities of two liver cancer cells comprising an in-vitro human liver cancer cell HepG2 and a rat liver cancer cell RH-35, the composition containing sulforaphen and oleanolic acid can substantially inhibit the growth of mouse metastasis tumors constructed by using the HepG2 cell, the composition containing sulforaphen and oleanolic acid has a certain specificity on the inhibition of the tumor cells, and the medicinal composition has on obvious influences on the growth of a normal rat liver cell BRL-3A under same concentration action, so the composition containing sulforaphen and oleanolic acid can be used in the liver cancer treatment medicines, can inhibit the tumor cells, and can also protect normal liver cells.
WO2011107283A3 Formulations of taurolidine and method for the production thereof The invention relates to a composition comprising taurolidine and/or the hydrolysis products thereof and also a biodegradable (co)polymer or inorganic matrix for use as an implant for treating local infections of the skeleton and soft tissue. A lozenge and a spray solution or gargling solution likewise comprises taurolidine and/or the hydrolysis products thereof and is used in the treatment of throat inflammations, sore throats with difficulty in swallowing, inflammations of the mouth and throat area and laryngitis. A method for producing taurolidine is also disclosed.
WO2014126596A1 Neuroprotective multifunctional antioxidants and their monofunctional analogs The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or -OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and -O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
EP1562955A1 Quinazoline derivatives as src tyrosine kinase inhibitors The invention concerns quinazoline derivatives of Formula (I): (A chemical formula should be inserted here - please see paper copy enclosed herewith) wherein Z is an O, S, SO, SO2, N(R2) or C(R2)2 group wherein each R2 group is hydrogen or (1-8C) alkyl, m is 0, 1, 2 or 3, each R1 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, n is 0, 1, 2 or 3, and each R3 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, or pharmaceutically-acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
US20080280995 Extracts of Latex of Calotropis Procera and to a Method of Preparation Thereof The invention relates to aqueous suspension of dried latex (DL) of Calotropis procera and to a method of preparation for the prevention/treatment of cancer. The DL suspension when administered orally in the X-myc mice—a transgenic mouse model of hepatocellular carcinoma (HCC), was effective in protecting the animals from the atypical mitosis and displastic/neoplastic changes occurring in vivo. Further, the DL suspension did not show any observable side effects when administered orally to the animals for 16 weeks. Further, the purified fractions of the latex were found to exhibit potent cytotoxic activity in in vitro cell culture system using two different cancer cell lines.
US20120302536 Use of DHEA Derivatives for Enhancing Physical Performance A method is disclosed for administering a DHEA derivative or a physiologically acceptable salt, ester or ether thereof for one of decreasing body weight, reducing adipose tissue, increasing endurance, as an anti-aging compound and generating production of red blood cells.
CN103524412A Isoquinolone derivative and synthetic method thereof The invention discloses a dihydroisoquinolone derivative with a structure as represented by a general formula (I). In the general formula (I) as described in the specification, R1 is a C1-4 alkyl group, and R2 is an amino group, an aminomethyl group, a carboxyl group or an aldehyde group. The invention further discloses a synthetic method for the derivative. According to results of experiments, the derivative has biological activity in vasodilatation, tumor inhibition, etc.
WO2010088842A1 Pharmaceutical compositions containing pyridyl cyanoguanidines, preparation methods and uses thereof The compositions formed from pyridyl cyanoguanidines and cyclodextrins, cyclodextrin derivatives and/or surfactants with solubilization, preparation methods and uses thereof.
WO2013142812A1 Antibacterial agents: sidechain-fluorinated myxopyronin derivatives The invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and G are as described in the specification, as well as compositions comprising a compound of formula I, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.
CN1864698A Capsule for treating gastric disease and preparation process thereof The present invention relates to Saiweian capsule and its preparation process. Saiweian capsule is used in treating gastric ulcer, duodenal ulcer, acute and chronic gastritis, esophagitis, stomatitis and other diseases. It is prepared with gypsum in 97-99 wt% and borneol in 1-3 wt%, and through grinding gypsum in kaoliang vinegar and sieving, crushing borneol and sieving, mixing and encapsulating. It has the functions of stopping bleeding, diminishing inflammation, astringing and promoting granulation to heal the ulcer surface.
CN102327601A Hemostat for resisting infection and promoting wound healing and preparation method thereof The invention relates to hemostat for resisting infection and promoting wound healing and a preparation method thereof. The produced hemostat adopts microporous starch as a main raw material, and every 100 grams of microporous starch contains 10 micrograms to 100 micrograms of antimicrobial and 5 micrograms to 50 micrograms of growth factor. Compared with traditional hemostat, the hemostat not only can rapidly and efficiently stanch, but also can diminish inflammation and resist the infection of the wound so as to accelerate the healing of the wound.
CN103315984A Applications of Fingolimod in preparation of drugs for inhibiting IL-6 secretion of hepatoma cells, The invention discloses applications of Fingolimod (code FTY720) in preparation of drugs for inhibiting IL-6 secretion of hepatoma cells, and belongs to the technical field of new use of drugs. In the application, through use of an ELISA method and through detection of expression situation of cytokine IL-6 in supernatants after Fingolimod (0 [mu]M-10 [mu]M) of different concentrations effects on SMMC-7721 and Huh7 cells, it is found that the Fingolimod can, on the dependence of doses, inhibit IL-6 secretion in the supernatants of the SMMC-7721 and Huh7 cells. The Fingolimod can be used for preparing drugs for inhibiting the IL-6 secretion of hepatoma cells, and has good development and application prospects. The applications of the Fingolimod in the preparation of drugs for inhibiting IL-6 secretion of the hepatoma cells are disclosed for the first time.
CN102670641A Liquid composition for contact lens The invention discloses a liquid composition for contact lens. The liquid composition comprises, in percentage by weight: about 1x10-5% to about 3% of vitamin, about 5x10%-3% to about 1% of a hydrophilic polymer, about 1x10-3% to about 1% of a surfactant, and a salt buffer.
CN1727015A Imipenem/cilastatin powder for injection, and transfusion preparation device of three chamber for dissolving dissolvants A thee-cavity injector for intravenous injection of the mixed solution of imipenem and cilastation features that it has three cavities for containing proportionally the solvent, imipenem powder and cilastatin powder respectively in relative cavity, and an openable partion is arranged between solvent cavity and two powder cavities. When it is used, the partition is opened to dissolving two powder medicines in the solvent.
CN103127122A Pharmaceutical composition of levodopa/folic acid compounds and purpose thereof The invention relates to a pharmaceutical composition of levodopa/ folic acid compounds and a purpose thereof, and belongs to the technical field of pharmacy. The pharmaceutical composition comprises the levodopa with medical dose, the folic acid compounds with the medical dose and a carrier which can be accepted in the pharmacy. The dose of the levodopa is 50-250 mg, and the dose of the folic acid compounds is 0.2-1.6 mg. The pharmaceutical composition of the levodopa/the folic acid compounds and the purpose thereof have the advantages of enhancing the curative effect of Parkinson disease resistance and improving the quality of life of a patient through the synergistic effect of multiple target points; being capable of effectively preventing and lowering the occurring risk of cerebral apoplexy of a Parkinson disease patient through a homocysteine (Hcy) target point; and in addition, enabling the patient to take medicine conveniently.
US20120213844 Liposome composition for targeting egfr receptor Short oligopeptides are provide which are capable of binding to the epidermal growth factor receptor on the surface of human tumor cells. Methods for using the peptides as targeting moieties in more complex compositions, such as conjugates of cytoxins, and/or structures, such as liposomal structures, for the purposes of drug delivery are also provided.
WO2014108452A1 Proteolysis targeting chimeras (protacs) directed to the modulation of the estrogen receptor A compound of formula (I): or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
CN101112377A Medicinal composition for treating avian mixed infection and method for preparing the same The present invention relates to a drug compound to treat the poultry mixed infection and the preparation method thereof, and the components and the mix ratios by weight of the drug component are 0.5 to 1.0 percent doxycycline hyclate, 10 to 20 percent metronidazole, 0.5 to 1.0 percent mequindox and 0.3 to 0.8 percent halofuginone respectively, while the rest is the excipients; the preparation method thereof is to smash and screen the raw materials of the drug, then the raw materials are mixed in line with the mix ratios and the excipients are added to 100 percent. The drug compound of the invention can be used for material mixing or drinking, which has easy usage, strong effects of anti-bacterial, anti-coccidiosis and anti-protozoa, etc., and good effects of prevention and treatment of a variety of mixed infection, small dosage, safety and low toxicity.
CN103720645A Thiocyanate erythromycin injection and preparation method thereof The invention relates to a thiocyanate erythromycin injection. A finished product of the thiocyanate erythromycin injection is prepared by the following steps: adding thiocyanate erythromycin into injection water, adding propylene glycol, adding Tween-80, fully stirring, finally generating a uniform liquid, and then performing constant volume, filtering and filling. Clinical tests show that the injection is stable in properties and stable in content after being stored for a long time, avoids adverse reactions to livestock with the injection, solves a problem that the absorptivity of a traditional orally-taken manner is lower, improves a curative effect and shortens a treatment cycle.
CN101991614A Compound fermented cordyceps sinensis powder (paecilomyces hepiali Cs-4 bacterial powder) combined medicine and preparation thereof The invention relates to a compound fermented cordyceps sinensis powder (paecilomyces hepiali Cs-4 bacterial powder) combined medicine, which is characterized in that: the medicine comprises the following raw material components in part by weight: 0.30 to 0.70 part of fermented cordyceps sinensis powder (paecilomyces hepiali Cs-4 bacterial powder), 0.45 to 0.90 part of disodium edetate, 0.05 to 0.10 part of ligustrazine phosphate, and 5.0 to 10.0 parts of water for injection (completely volatilized when dried); a preparation method of the compound fermented cordyceps sinensis powder (paecilomyces hepiali Cs-4 bacterial powder) combined medicine comprises the steps shown in the specifications; the compound fermented cordyceps sinensis powder (paecilomyces hepiali Cs-4 bacterial powder) combined medicine can be prepared into capsules, granules or tablets according to pharmaceutically acceptable dosage; and the combined medicine has new application, namely is used for resisting ageing, fatigue, shock and anoxia and improving immunity.
WO2010124695A1 Use of griseofulvin for the improvement of mental faculties: attention, concentration and memory The invention relates to the pharmaceutical substance griseofulvin, which has the following formula and chemical structure: C17H17ClO6, (2S,6'R)- 7-chloro- 2',4,6-trimethoxy- 6'-methyl- 3H,4'H-spiro [1-benzofuran- 2,1'-cyclohex[2]ene]- 3,4'-dione. Said substance is extracted from solutions of Penicillium patulum obtained by fermentation. The substance has the following references: GB 784,618 (Glaxo; appl. 28.3.1955). US 2,900,304 (ICI; 18.8.1959; GB-prior. 21.9.1956). US 3,038,839 (Glaxo; 12.6.1962; GB-prior. 2.3.1959). US 3,069,328 (Glaxo; 18.12.1962; GB-prior. 4.5.1960). US 3,069,329 (Glaxo; 18.12.1962; GB-prior. 4.5.1960). Said substance, which is generally administered orally at present, is used for treating decline and disorders of the mental faculties: attention, concentration and memory.
WO2008001885A1 Abl KINASE INHIBITOR Disclosed is an Abelson kinase (Abl kinase) inhibitor containing an indazole derivative represented by the formula (I) below or a pharmacologically acceptable salt thereof as an active ingredient. Also disclosed is an Abl kinase inhibitor containing an indazole derivative represented by the formula (Ia) below or a pharmacologically acceptable salt thereof as an active ingredient. (I) [In the formula (I), R1 represents a substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group.] (Ia) [In the formula (Ia), R2 represents CONR4aR4b (wherein R4a and R4b may be thesame as or different from each other and represent a hydrogen atom or a substituted or unsubstituted lower alkyl, or alternatively R4a and R4b may form a substituted or unsubstituted heterocyclic group together with an adjacent nitrogen atom) or the like, and R3 represents a hydrogen atom, a substituted or unsubstituted lower alkyl or the like.]
CA2369099C Anticonvulsant derivatives useful in reducing blood glucose levels Use of anticonvulsant derivatives of formula (I) for reducing blood glucose levels, wherein X is CH or oxygen; R1 is hydrogen or alkyl; and R2, R3, R4 and R5 are independently hydrogen or alkyl and, when X is CH2, R4 and R5 may be alkene groups joined to form a benzene ring and, when X is oxygen, R2 and R3 and/or R4 and R5 together may be a methylenedioxy group of formula (II), wherein R6 and R7 are the same or different and are hydrogen, or alkyl and are joined to form a cyclopentyl or cyclohexyl ring.
CN102688191A Medicine composition containing vitamin K1 and oil The invention relates to a medicine composition containing vitamin K1 and oil. Concretely, the medicine composition comprises 1 part of vitamin K1 by weight and 10-2,000 parts of oil by weight; and the iodine value of the composition is less than 1.0, and the saponification value is 310-360. The medicine composition containing vitamin K1, provided by the invention, can be orally taken, has good pharmaceutical characteristics and can be applied to wider population including infants.
CA2197210C Intravenous alendronate formulations Disclosed is a therapy protocol for treating patients having metastatic bone disease, hypercalcemia of malignancy and/or metabolic bone disease by administering an intravenous, citrate-buffered formulation of alendronate which is isotonic with human blood.
CN101897675B Solid oral medicinal composition containing valsartan or pharmaceutically acceptable salts of valsartan The invention relates to a solid oral medicinal composition containing valsartan or the pharmaceutically acceptable salts thereof. Particularly, the composition is directly prepared into particles by a wet method according to a new formula.
US20090130193 Methods of Treating Cancer with High Potency Lipid-Based Platinum Compound Formulations Administered Intraperitoneally One aspect of the invention relates to methods of treating cancer in a patient comprising administering intraperitoneally to a patient in need thereof a cancer treating effective amount of a composition comprising a lipid-complexed platinum compound wherein the concentration of the platinum compound of the lipid-complexed platinum compound composition is greater than about 1.2 mg/ml. Another aspect of the invention relates to lipid-complexed platinum compound compositions where the concentration of the platinum compound is greater than about 1.2 mg/ml.
CN101747215A Method for preparing meclofenoxate hydrochloride sterile bulk drug The invention relates to a method for preparing a meclofenoxate hydrochloride sterile bulk drug, which is characterized in that a meclofenoxate hydrochloride sterile finished product is obtained by the following steps: dissolving meclofenoxate hydrochloride in isopropanol in a certain mixture ratio, then decoloring and carrying out aseptic filtration and decompression concentration, and then devitrifying, filtering and drying. The product prepared by the method has more stable quality and simple process, thereby being suitable for industrial big production.
US20080279932 Vildagliptin salt; in mixture with therapeutic agents such as antidiabetic agents; antilipemic agents; obesity; appetite control; hypotensive agents; cholesterol absorption moderators; anticoagulants; estrogen receptor moderators; transferring across blood-brain barrier The present invention relates to novel salt forms of vildagliptin (LAF237), i.e. salt forms of(S)-1-[(3-hydroxy-1-adamantyl)amino]acetyl-2-cyano-pyrrolidine.
US20080255086 Heterocyclic Derivatives The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
CN103214479A Pyrazole naphthylurea tyrosine kinase inhibitor and its application The invention relates to a pyrazole naphthylurea tyrosine kinase inhibitor. The pyrazole naphthylurea tyrosine kinase inhibitor is compounds having structures represented by general formula I, and medicinal salts thereof. The compounds have tyrosine kinase inhibition activities, and can be used in medicines for treating tyrosine kinase mediated diseases or illnesses as a tyrosine kinase inhibitor.
CN1720238B Neurologically-active compounds The present invention relates to neurologically-active compounds. Also disclosed are processes for the preparation of these compounds and their use as pharmaceutical or veterinary agents, in particular for the treatment of neurological conditions, more specifically neurodegenerative conditions such as Alzheimer's disease.
CN101897715A Nuezhenoside and rhoifolin composition and use thereof in preparation of drugs The invention relates to a nuezhenoside and rhoifolin composition, which is prepared by mixing 20%-80% by weight of nuezhenoside with 80%-20% by weight of rhoifolin, the composition can be used for preventing and treating influenza as a neuraminidase inhibitor and be prepared into pharmaceutically acceptable formulations.
WO2009026816A1 The application of 1-aryl-2(1h)-pyridone compounds in preparation of medincines for treating itching of the skin The pharmaceutical application of 1-aryl-2(1H)-pyridone compounds, especially the application of 1-aryl-2(1H)-pyridone compounds in preparation of medicines for treating itching of the skin. The 1-aryl-2(1H)-pyridone compounds used to treat itching of the skin are administrated topically.
EP2776396A2 Heteroaryl hydroxamic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or dsasiereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
CA2853152A1 Compositions and methods for treating vaginal infections and pathogenic vaginal biofilms The present invention generally relates to methods and compositions for treating pathogenic vaginal biofilms. More specifically, the invention relates to pharmaceutical compositions comprising a combination of boric acid and diethylaminetetracetic acid (EDTA) and to methods of using such compositions to treat or prevent biofilm formation associated with vaginal infections, such as bacterial vaginosis (BV), vulvovaginal candidiasis (VVC), trichomoniasis or mixed infections.
US7112594 A N-phenyl-benzo(b)thiophene-carboxamide derivatives, as enzyme inhibitor of tyrosine kinase; antiproliferation of lymphocyte, treating autoimmune disease, rheumatic disease, as immunosuppressant, antiinflammatory agents Compounds represented by the following general formula (I) wherein ring A is benzene, cyclohexane, pyridine, piperidine, a derivative thereof, imidazole, a derivative thereof, etc.; the ring B represents benzene, cyclohexane, pyrrole or a derivative thereof, furan, thiophene, etc.; R1, R2 and R3 represent each hydrogen, alkyl, halogen, hydroxyl, alkoxy, etc.; W represents hydrogen, alkyl or hydroxycarbonylalkyl; X represents halogen, cyano, nitro, etc.; X′ represents hydrogen, halogen, etc.; and Y represents alkyl, hydroxyalkyl, hydroxycarbonylalkyl, aminoalkyl, etc.; salt thereof, and drugs comprising these compounds. Because of having an exellent effect of inhibiting activated lymphocyte proliferation, these compounds are usefull as preventives or remedies for various autoimmune diseases.
WO2006077026A1 2, 5-disubstituted phenyl methanone derivatives as glycine transporter 1 (glyt-i) inhibitors for the treatment of neurological and neuropsychiatry disorders The present invention relates to compounds of the general formula (I) wherein R1 is -OR1 , -SR1 or is a heterocycloalkyl group; R1 is lower alkyl, lower alkyl substituted by halogen, or is -(CH2)n-cycloalkyl; R2 is -S(O)2-lower alkyl or -S(O)2NH-lower alkyl; R3 is aryl or heteroaryl, which are unsubstituted or substituted by one to three substituents, selected from the group consisting of lower alkyl, lower alkoxy, CN, NO2, -C(O)-lower alkyl, -C(O)O-lower alkyl, halogen or lower alkyl substituted by halogen; n is 1 or 2; m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GIyT-I).
WO2011034896A3 Small molecule inhibitors of the alpha4-paxillin interaction The present invention is directed to novel compounds that are able to inhibit the interaction of paxillin or its paralogues, including leupaxin or Hic-5f with alpha.4 integrin or its binding partners that regulate signaling events downstream of the paxillin~,alpha.4 interaction, The present invention further relates to methods for therapeutic use of such compounds and pharmaceutical compositions of such compounds for the treatment of a disease or condition.
CN102973640A Radix astragali-radix pseudostellariae tea The invention relates to radix astragali-radix pseudostellariae tea. The radix astragali-radix pseudostellariae tea is composed of 8-12 g of radix astragali, 8-12 g of radix pseudostellariae and 100-200 mg of vitamin C. The radix astragali-radix pseudostellariae tea is prepared by the steps of weighing each component of the raw material drugs according to the weight proportion, grinding into fine powder respectively, mixing the powder, loading the mixture in tea bags. The radix astragali-radix pseudostellariae tea has the function of hypoxia tolerance, and is convenient to take, without any toxic and side effect.
CA2393883C Salicylamide derivatives Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-.kappa.B with little side effects.
US20120129902 4-SUBSTITUTED-3-PHENYLSULFANYLMETHYL-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.
US20090196862 High dosage Vitamin D A preparation containing vitamin D3 (cholecalciferol), preferably an edible oil, in an amount of 200 IU to 20,000 IU, preferably 1000 IU to 5000 IU, and most preferably about 1500 IU to 3500 IU, with about 2000 IU particularly preferred. Such a preparation is useful in providing adequate nutrition, in the prevention and/or treatment of Seasonal Affective Disorder (SAD), fall prevention, multiple sclerosis, chemoprevention of cancer, accelerated fracture healing, and metabolic syndrome. It acts as an anti-depressant, an anti-hypertensive for renovascular hypertension and high-renin hypertension; and is useful in hyperlipidemia treatment, as well as in the treatment of hypovitaminosis D in the renal failure population. The most important application to the present inventors is in treatment, prevention and also reversal of hypertension in renovascular and high-renin hypertension. The effective amount of vitamin D, based on blood serum content, is equal to or greater than 20 ng/mL, preferably equal to or greater than 40 ng/mL, and most preferably equal to or greater than 50 ng/mL, with no specific upper range, but preferably equal to or less than 200 ng/mL, and more preferably equal to or less than 100 ng/mL.
US20090137629 Sigma receptor binding agent containing indanone derivative A method for treatment of a mental disorder containing the step of administering a therapeutically effective amount of a sigma receptor binding agent containing an indanone compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. The variables of formula (I) are recited in the present specification.
WO2009137782A2 Allosteric enhancers of the a1 adenosine receptor The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.
US7105538 4-oxo-4-[2-(5-pyridin-4-yl-[1,3,4]oxadiazol-2-yl)-pyrrolidin-1-yl]-butyric acid ethyl ester; inhibition of serotonin re-uptake; analgesic effect Substituted 2-pyrrolidin-2-yl compounds corresponding to formula I a method for their production, pharmaceutical compositions containing them, and methods of using them, especially for treating pain and/or depression.
CN101721420A Antishock function of ginsenoside Re The invention belongs to the technical field of medicines, and discloses an antishock function of ginsenoside Re. The ginsenoside Re has favorable treatment effects on haemorrhagic shock, infectious shock, scalding shock and hypoglycemic shock. According to a test result, the minimum effective quantity of the ginsenoside Re is 40mg/kg, and LD 50 is 400mg/kg. The ginsenoside Re can be mixed with a pharmaceutically acceptable carrier to prepare various clinically-acceptable dosage forms such as tablets, capsules, injection, granule and the like so as to improve a shock state and reduce the death rate of shocking animals. The invention can be clinically applied to shock rescue, generates an assisted antishock function and improves the success rate of the shock rescue.
US6846843 β-thioamino acids Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.
US7598244 (S)-1-(3-ethoxy-1-methylpropyl)-3-[7-(3,4-methylenedioxyphenyl)-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl]urea; preventive and/or therapeutic agent for immunological rejection and/or graft versus host reaction in organ/bone marrow transplant, autoimmune disease, allergic disease and/or inflammatory disease Novel [1,2,4]triazolo[1,5-a]pyrimidine derivative of the general formula (1): (1) its prodrug or a pharmaceutically acceptable salt thereof, which exhibits an antigen presentation inhibiting activity and is useful as a preventive and/or therapeutic agent for immunological rejection and/or graft versus host reaction in organ/bone marrow transplant, autoimmune disease, allergic disease and/or inflammatory disease and also useful as an anticancer drug or as an immunological tolerance inducer for transplanted organ/transplanted bone marrow.
US7169778 Antiproliferative agents; anticancer agents; central nervous system disorders; antiarthritic agents Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3–7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The present invention also provides a method of treating cell proliferative disorders. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).
WO2013185933A1 Pharmaceutical composition for liver regeneration A pharmaceutical composition for use in a method for liver regeneration or for increasing liver performance contains vitamins B6, B9 and B12 in the daily dosages: B6 not less than 4 mg, optionally not more than 500 mg; B9 not less than 0.6 mg, optionally not more than 15 mg; B12 not less than 0.008 mg, optionally not more than 4 mg.
US7323458 Dihydrobenzodiazepins and their use for treating dyslipidemia The invention concerns a benzodiazepin derivative of formula (I) and their use for treating dyslipidemia, atherosclerosis, diabetes and its complications.
US20110065753 Methods of treating poxviral infections Provided are methods of treating a disease or condition caused by or associated with a virus belonging to the Poxyiridae family using iminosugars, such as DNJ derivatives.
EP0794793B1 Composition for prevention and treatment of hiv-1 infection comprising at least two different hiv-1 reverse transcriptase inhibitors A composition and method for the prevention or treatment of HIV-1 infection comprising an HIV-1 reverse transcriptase-inhibiting hterocyclyl carb(ox/thio)anilide compound, a second HIV-1 reverse transcriptase inhibitor compound which does not select for the same HIV-1 mutant strain or strains selected for by the heterocyclil carb(ox/thio)anilide compound, and, optionally, a thrid HIV reverse transcriptase inhibitor compound.
CN103751130A Amlodipin dispersible tablet and preparation method thereof The invention provides an amlodipin dispersible tablet. The amlodipin dispersible tablet is prepared by the following steps of: dispersing amlodipin in a water-soluble matrix; and adding a suitable excipient to prepare the dispersible tablet, wherein the amlodipin can be solvate, ester or medicinal salt of amlodipin, and the water-soluble matrix is selected from polyethylene glycol, povidone, poloxamer and carbohydrates. The amlodipin dispersible tablet effectively covers up the bitter taste of the amlodipin and can be used for preparing antihypertensive medicaments.
CN101138548A Polyglycol derivatization phospholipid loaded vinorelbine nano-micelle preparations The present invention provides a nanometer micelle of the vinorelbine preparation for the vein injection, which comprises the vinorelbine of effective amount, the polyethylene glycol-phospholipid and the adjuvant accepted in pharmacy. The nanometer micelle of the vinorelbine preparation for the vein injection is prepared by packaging the vinorelbine into the nanometer micelle. The nanometer micelles with uniform diameter are formed by the vinorelbine and the polyethylene glycol-phospholipid. In the micelle, the hydrophobic core of the vinorelbine is packaged by the carbowax molecule; therefore an inhibitory coating with hydrophilicity is formed. The contaction between the vinorelbine and the enzyme protein molecule in the blood is avoided. The vinorelbine is protected from identification and swallowing by the endothelial system. The circulating time of the medicine in the body is prolonged. In addition, the micelle improves the storing actability and the anti-tumor effect of the vinorelbine. The toxicity of the vinorelbine is reduced.
CN1907260A Hydrocortisone clyster agent and method for preparing the same The invention discloses a loosening enema and preparing method of kao hydrate, which comprises the following parts in each 6000ml: 9.0-11.0g kao hydrate, 11.6-14.2g Tween-80, 81.0-99.0g CMC-Na, 2.1-2.7g aethylum hydroxybenzoicum and pure water. the preparing method comprises the following steps: allocating 7.2-8.8% Tween-80; stirring; dissolving; adding kao hydrate to stir evenly; allocating 4.5-5.5% aethylum hydroxybenzoicum; boiling; adding CMC-Na; bulking; adding purified water to stir evenly.
CA2326662C Therapeutic system which can be moisture-activated The invention relates to a therapeutic system for the temporal and controllable administering of at least one therapeutic active substance to a human or animal organism by means of diffusion through the skin or a mucous membrane. The active substance is initially available in a first state for production and storage. In this state, the active substance is chemically stable and is insufficiently permeable for the skin or a mucous membrane. The active substance is transformed into a second state at the application site when exposed to moisture. In said second state, the active substance is suited for diffusing through the skin or a mucous membrane, and is absorbed into the organism. The invention is characterized in that, in a first state, the active substance is contained as a pharmaceutically acceptable salt in the system. The salt is chemically transformed into the second state of an acid or base by exposure to water and by an active agent also contained in the system. Compared to the salt, the acid or base is absorbed into the organism through the skin or a mucous membrane in an accelerated and increased manner. Said active agent is a solid substance which reacts in an aqueous solution in an acidic or basic manner or is a mixture of a plurality of such substances. This active agent has a proportion of water of at least 5 % in the solid body structure thereof or is bonded thereto.
US20120017924 Coated nicotine-containing chewing gum, manufacture and use thereof A coated chewing gum product for the delivering of nicotine in any form to a subject by a rapid transmucosal uptake in the oral cavity comprising at least one gum core, nicotine in any form and/or a nicotine mimicking agent, at least one coating layer and optionally at least one or more other additive, wherein said at last one coating layer is buffered. Also contemplated is a method for the delivering of nicotine in any form, a method for the reduction of the urge to smoke or use tobacco as well as a method for producing said coated chewing gum and the use of the same form obtaining a quick transmucosal uptake of the nicotine in the oral cavity of a subject.
US20100015234 Pharmaceutical preparations and their manufacture A method for making a composition comprising active particles comprising an active substance comprises the steps of a) providing an emulsion having a dispersed phase comprising a solution of the active substance in a solvent and b) inducing the formation, in the emulsion, of solid particles comprising the active substance. The particles may be isolated from the emulsion. Active particles having a normalized kurtosis of at least 5 and a mean diameter of less than 100 μm are provided.
US20130065873 Metal complexes The present invention relates, inter alia, to metal complexes having improved solubility, process for the preparation of the metal complexes, devices comprising these metal complexes, and the use of the metal complexes.
CN102988355A Application of Aphanamixoid A for preparing helicobacter pylori resistant medicine In-vitro activity experiments show that Aphanamixoid A has strong helicobacter pylori (Hp) resistant activity. Aphanamixoid A can be used for treating diseases, such as acute and chronic gastritis, gastric ulcer, duodenum ulcer and the like and applied for preparing medicines for treating acute and chronic gastritis, gastric ulcer and duodenum ulcer. The application of Aphanamixoid A for preparing the helicobacter pylori resistant medicine is disclosed for the first time; because the skeleton type belongs to a brand new skeleton type and the helicobacter pylori inhibitory activity of Aphanamixoid A is strong unexpectedly, the possibility that other compounds give any inspiration does not exist; Aphanamixoid A has outstanding substantive characteristics; and simultaneously, Aphanamixoid A has obvious progress for preventing and treating helicobacter pylori infection.
CN1565455A Antibiotics compositions for curing broad spectrum beta-lactamase bacteria infection The invention relates to an antibiotics compositions for curing broad spectrum beta-lactamase bacteria infection, comprising cefepime and Tazobactam, whose weight ratio is 20:1-1:2.
US6935334 Enhancing therapeutic effectiveness of nitric oxide inhalation Methods for reducing, partially preventing or completely preventing nitric oxide (NO) inhalation-related impairment of HPV in a mammal are disclosed. The methods include administering a therapeutically effective amount of NO by inhalation, and co-administering an effective amount of an anti-reactive oxygen species (anti-ROS) agent, e.g., N-acetyl-cysteine, or a leukotriene blocker. Methods for reducing, partially preventing or completely preventing loss of pulmonary vasodilatory responsiveness to NO inhalation in a mammal are also disclosed. The methods include administering a therapeutically effective amount of NO by inhalation, and co-administering an effective amount of an anti-ROS agent a therapeutically effective amount of a leukotriene blocker.
CN101708180A Enterotoxemia Weak-neomycin sulphate The invention discloses an enteromtoxemia Weak-neomycin sulphate without side effect for many raisers, comprising the following components by weight: 5-20 g of neomycin, 2-12 g of substituted nitramisole, 0.05-0.5 g of diclazuril, 100-500 mg of K3, 50-150 mg of atropine and 70-90 g of anhydrous dextrose. The production process comprises the following steps of: putting the components according to the weight proportion in a three-dimensional mixer to primarily mix for 10-15 minutes at the temperature of 25 DEG C and the humidity of no higher than 30, and then adding a carrier to mix for 20 minutes, after mixing, filling in aluminum foil bags or plastic bottles as soon as possible, and finally sealing and packaging.
US20100099680 Pteridinone derivatives as p13-kinases inhibitors New compounds of Formula (1) are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.
US20120294933 Use of PVP-Iodine Liposomes for Treatment of Acne The invention concerns a method for the production of a pharmaceutical preparation for the treatment of acne forms that is characterized in, that the preparation comprises at least one antiseptic compound associated with a particular carrier.
CN1850850A 17a-oxa-D-carburated 5 alpha-androstane-17-one-3beta-alcohol ester, and its preparing method and use The invention relates to PPAR alpha/beta/gama triplication excitant active 17a-oxa-D-carburet-5 alpha-sterane-17 ketone-3 beta-alcohol ester. The manufacture method is that adopts 5 alpha-sterane-17 ketone-3 beta-alcohol ester dissolving in chloroformic solution containing inter-chlorine benzoper acid to reacting for 2-6 days, after extracting, column chromatography, recrystallization, the high purity 17a-oxa-D-carburet-5 alpha-sterane-17 ketone-3 beta-alcohol ester would be gained. The invention could be used to cure 2-type diabetes.
CN101257800B Medicaments containing famotidine and ibuprofen An oral dosage form for administration of ibuprofen to a subject in need of ibuprofen treatment is provided, in which an oral dosage form comprising a therapeutically effective amount of ibuprofen and a therapeutically effective amount of famotidine, in admixture, in amounts suitable for three times per day administration.
US7217714 1-(3-carboxamido-3-phenylpropyl)piperidin-4-yl -triazole or oxazole derivatives, for treatment and prevention of infection by HIV-1 and genetically related retroviruses Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ] (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.
CN103638523A Medicinal composition containing donepezil or its pharmaceutically acceptable salt and beta-receptor blocker The invention relates to a medicinal composition, which comprises: an acetylcholinesterase inhibitor donepezil, selectively a pharmaceutically acceptable salt; and a beta-receptor blocker and a medicinal carrier. The medicinal composition provided by the invention is suitable for treatment of vascular dementia.
CN101342265A Instant jelly glue of musk deer bead for eyes The present invention discloses an immediate eye gel which is made of moschus bead and is used for improving the eyesight, and a preparation method thereof. The immediate eye gel of 1000 milliliters comprises 72 grams of pearl, 1.2 grams of moschus, 6 grams of caterpillar fungus, 3 grams of shell of abalone, 3 grams of Chinese goldthread, 3 grams of corktree, 3 grams of rhubarb, 3 grams of borneol, 0.6 gram of snake gall, 0.6 gram of extract of pig gall, 3 grams of calamine, 6 grams of leaf of perilla, 6 grams of schizonepeta, 0.05 to 1 gram of preservative, 1.0 to 7.5 grams of osmotic pressure regulator, 30 to 150 grams of gel matrix, pH buffer and water for injection. The immediate eye gel improves the optimization and technology of supplementary materials, enriches the pharmaceutical dosage forms of the eyesight improving moschus bead, greatly prolongs the residence time of medicine on eyes, enhances the curative effect, and has no adverse stimulating reaction.
WO2008076042A1 Azetidinpiperazine derivatives that are neurokinin (nk) receptor antagonists and their use. The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising said compounds, and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of compounds of formula (I).
CA2230947C Implantable controlled release device to deliver drugs directly to an internal portion of the body A simple and implantable sustained release drug delivery device with an inner core containing an effective amount of a low solubility agent covered by a non-bioerodible polymer coating layer that is permeable to the low solubility agent is disclosed. A method for treating a mammal to obtain a desired local or systemic physiological or pharmacological effect by surgically implanting such a sustained release drug delivery device into a mammal in need of treatment is also disclosed.
WO2010128446A1 Novel acylated 1,6-anhydro decasaccharide and its use as antithrombotic agent The instant invention relates to the decasaccharide of Formula (I), wherein Ac represents an acetyl group: in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of Formula (I) is useful as an antithrombotic agent.
US20110245154 Methods and Compositions for Treating Viral or Virally-Induced Conditions Provided are methods and compositions for the prevention and/or treatment of viral conditions, virally-induced conditions and inflammatory conditions. The methods can comprise administering to a subject a viral inducing agent with an antiviral agent, and optionally an additional agent. The viral inducing agent can be a HDAC inhibitor administered orally.
WO2013173519A1 Beta-lactamase substrates and methods of their use for the diagnosis of tuberculosis β-Lactamase substrates and methods for using the substrates to detect β-lactamase diagnose tuberculosis.
US20080214594 Inhibitors Of Checkpoint Kinases The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
CN102671154A External application powder for treating diseases of cervical vertebra The invention discloses external application powder for treating diseases of cervical vertebra, and relates to Chinese patent medicines. The external application powder has efficacy of dispelling the wind and cold, removing dampness, promoting blood circulation and stimulating the menstrual flow to remove blood stasis, relieving swelling and pain and dissolving bone spurs, and promotes tissue regeneration while promoting blood circulation to remove the stasis. The external application powder has the advantages that the external application powder is pollution-free, and is not prepared at high temperature, active ingredients of the powder are not destroyed by high temperature, the external application powder is free of lead poisoning, fire toxin and side effects, and is easily absorbed, the active ingredients of the powder directly reach the focus of infection of a patient after permeation and bypass the liver and the kidneys of the patient, the original pharmaceutical effects of the powder are kept, accordingly utilization rate of the powder is increased, the dosage of the powder is centralized, effects of the powder are everlasting, the bone spurs are softened, further growth of the bone spurs is suppressed, the powder is anti-inflammation, repercussive and demulcent, and the purpose of treating hyperosteogeny which is cervical spondylosis.
CN1823819A Food and medicine dual purpose product for preventing and treating vision injury syndrome duo to TV and computer display light and its manufacturing method A Western medicine used as both medicine and food for preventing and treating vision syndrome caused by computer and television set, such as xerophthalmia, eye strain, blurred vision, hypomnesia, cervical pain, etc, is prepared from vitamins and trace elements. Its preparing process is also disclosed.
US7514426 Substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl, benzyl, cyano, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is lower alkyl substituted by halogen; R3 is hydrogen, methyl or aryl; R is lower alkyl, cycloalkyl or aryl; and pharmaceutically acceptable acid addition salts thereof.
US20090036362 Angiogenesis Affecting Polypeptides, Proteins, and Composition, and Methods of Use Thereof The present invention relates to polynucleotides and proteins associated with vasculogenesis- and angiogenesis-related disorders. The invention further relates to methods for the identification of compounds that modulate the expression of angiogenesis-related genes and gene products and to using such compounds as therapeutic agents in the treatment of angiogenesis-related disorders. The invention also relates to methods for the diagnostic evaluation, genetic testing and prognosis of angiogenesis-related disorders, and to methods and compositions for the treatment these disorders.
CN101974011B New compound methyl brevicate with medical activity The invention relates to a new compound with a structural formula (I). The compound can be extracted and separated from the dry complete grass of Erigeron Breviscapus (Vant.) Hand.-Mazz. The compound has the effects of inflammatory reaction resistance, platelet aggregation resistance, thrombus resistance and blood vessel extension and can be used for preparing a medicament for treating a heart cerebrovascular disease. The structural formula (I) is shown in the specification.
CN101229353A Medicine compounds for treating rheumatoid and atrophic arthritis The invention provides a drug combination for curing rheumatoid arthritis and atrophic arthritis, which is a preparation prepared by the following raw materials by weight ratio: 1-9 portions of turmeric and 9-1 portions of cassia bark. The invention also provides a preparation method of the drug combination and an application thereof. The drug combination of the invention can cure the rheumatoid arthritis and the atrophic arthritis with precise efficacy; furthermore, the turmeric and the cassia bark are used compatibly, which improves the function of lucrative synergies and provides a new choice for the clinical application.
WO2005073236A3 Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors The invention relates to the compounds of formula (I), which are suitable for producing drugs for the prophylaxis and therapy of diseases, whereby the course thereof involves the increased activity of matrix metalloproteinases. Diseases belonging thereto are degenerative joint diseases, for example, osteo-arthroses, spondyloses, chondroporosis after articulation injury or a long duration of articulation immobilization after meniscus or patella injury or torn ligaments, or a disease of the connective tissue, such as collagenoses, periodontal diseases, problems with healing wounds, or a chronic disease of the locomotor system, such as inflammatory, immunological or metabolic-related acute or chronic arthrites, arthropathies, myalgies or troubles of the bone metabolism, or ulceration, atherosclerosis or stenosis. The compounds of formula (I) are also suitable for treating inflammatory diseases or cancers, metastatic tumors, cachexia, anorexia, heart failure or septic shock and in the prophylaxis of myocardial and cerebral infarction.
EP1062954B1 Use of itaconic acid for regulation of glycolytic metabolism Foods and drinks containing an effective amount of fructose 6-phosphate-2 kinase inhibitors which are safe and efficacious in vivo (for example, itaconic acid) and medicinal compositions containing the inhibitors as the active ingredient. These foods, drinks or medicinal compositions exhibit an obesity-preventive effect, an anti-diabetic effect and an anti-hyperlipemic effect while showing a high safety and no pain.
US20090291905 Fungal phytotoxin fusicoccin for the treatment and diagnosis of coagulation-correlated pathologies The present invention concerns the use of tricyclic terpenes chosen from the group consisting of fusicoccin, ophyobolins or cotylenins for the therapy and diagnosis of coagulation-correlated pathologies such as Bernard-Soulier syndrome (BSS), von Willebrand disease (vWD), Glanzmann's thrombasthenia or thrombocytopenia.
US7022860 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10 -dioxo-2H-1,2,3-triazolo(4,5-c)(1)benzazepine, for example; chemical intermediates, synthesis using relatively inexpensive reagents A process for preparing a compound represented by formula (IIa′) wherein Q represents group (i) as defined in the specification and R2 to R5, R31, R32, and R52 are as defined in the specification, by (1) reacting a compound represented by formula (V) wherein R2 to R5 and R52 are as defined in the specification. with a compound represented by R31R32C═O wherein R31 and R32 are as defined in the specification; (2) reacting the compound prepared in (1) with a compound represented by R71—C(═O)—R72 wherein R71 and R72 each independently represent a chlorine atom, 4-nitrophenyl, or 1-imidazolyl; and (3) reacting the compound prepared in (2) with a compound represented by R33OH wherein R33 is as defined in the specification.
CN101913992A Preparation method for polyprenol obtained by rapid medium-pressure column separation and anti-H3N2 virus injection The invention discloses a preparation method for polyprenol obtained by rapid medium-pressure column separation and an anti-H3N2 virus injection. A fat-soluble unsaponifiable matter of which the polyprenol content is less than 40 percent is used as a raw material; active carbon and attapulgite are used as a mixed decoloring agent; the mass ratio of the active carbon to the attapulgite is 1:(1 to 20); the mass ratio of the decoloring agent to the crude product of polyprenol is (10 to 150):100; and 90 percent polyprenol is obtained by mixing the decoloring agent and the raw material at the temperature of between 50 and 120 DEG C to decolor for 10 to 80 minutes and performing medium-pressure column chromatography separation on the decolored polyprenol. The polyprenol can be used for developing a new medicament for preventing the attack of H3N2 influenza A virus. Compared with the conventional purification method, the method has the advantages of high yield, convenience, economy, suitability for industrial production and the like.
EP1227086B1 1-substituted phenyl-1-(1h-imidazol-4-yl) alcohols, process for producing the same and use thereof [Object] To provide compositions which have a steroid C17,20 lyase inhibitory activity and are useful as preventives and/or remedies for tumors such as prostatism and mammary cancer. Compounds represented by general formula (I) or salts thereof have a steroid C17,20 lyase inhibitory activity and are useful as preventives and/or remedies for tumors such as prostatism and mammary cancer. In said formula R represents hydrogen or a protective group; R1 represents lower alkyl or cyclic hydrocarbyl; R2 represents optionally substituted aryl or optionally substituted heteroaryl; R3 represents optionally substituted hydrocarbyl, optionally substituted hydroxy, optionally substituted thiol, optionally substituted amino, acyl or halogeno; and n is an integer of from 0 to 4.
CN102100682A Slow release long-acting rasagiline transdermal patch with high bioavailability and preparation method thereof The invention relates to a slow release long-acting rasagiline transdermal patch with high bioavailability and a preparation method thereof. The patch is characterized in that effective amount of rasagiline and a substrate are contained, wherein the concentration of rasagiline is in the range of 0.1 mg/cm2 - 2 mg/cm2, every patch contains 1 mg - 10 mg of rasagiline, and the substrate contains one or more than two kinds of the following substances: acrylic polymers containing no carboxylic group and silicone polymers with silanol groups capped by alkyls. The time of maximum plasma drug concentration of the patch is prolonged to be 5 times or more that of oral tablets, and the bioavailability of the patch is 130 percent or more of that of oral tablets. The patch in the invention can be applied to effectively inhibit monoamine oxidase B (MAOB) for at least 3 days, in addition, the preparation method is simple and suitable for industrial production.
WO2005035503A1 Novel isoquinoline derivative To prepare a novel isoquinoline derivative useful as a subject medicine and to find out a new pharmacological activity of the derivative. The compound is represented by the general formula [I] and has excellent Rho-kinase inhibitory activity. In the formula, X represents a benzene ring or monocyclic aromatic heterocycle; Y represents the general formula (a), (b), (c), (d), (e), or (f); R1 and R2 each represents hydrogen or alkyl; and R3 and R4 each represents halogeno, hydrogen, OH, alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy, cycloalkenyloxy, aryloxy, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, carboxy, hydrocarbonyl, alkylcarbonyl, arylcarbonyl, amino, alkylamino, arylamino, mercapto, alkylthio, arylthio, etc., provided that the groups may be substituted.
EP2561868A1 Pharmaceutical compositions comprising hydroxychloroquine (HCQ), Curcumin, Piperine/BioPerine and uses thereof in the medical field The present invention concerns a pharmaceutical composition containing HCQ, curcumin and BioPerine/piperine and its application in the medical field. In particular, the composition according to the invention can be advantageously employed in the prevention or treatment of a subject presenting with a proliferative disorder, to slow the progression of and/or or to cause regression of a premalignant plasma cell proliferative disorder like a monoclonal gammopathy of undetermined significance (MGUS) and/or smoldering (asymptomatic) multiple myeloma (SMM) and/or Indolent multiple myeloma (IMM) and/or to cause remission of a cancer arising from a premalignant plasma cell proliferative disorder like multiple myeloma (MM).
CN101917989A Preparation containing chromane-2-one derivatives The invention relates to preparations containing at least one compound of the formula (I), wherein the substituents R1 - R4 have a meaning disclosed in Claim 1, and to the salts and solvates thereof, and to the use thereof, and to selected compounds of the formula (I).
US20080039367 Medicinal Composition Containing Diabeted Remedy A pharmaceutical composition effective for the prophylaxis and treatment of diabetes is provided. This pharmaceutical composition comprises the combination of an α-amylase inhibitor selected from a compound represented by the following general formula (I): [wherein A represents, for example, a cyclic group, etc. R1 and R2 represent an alkyl group, hydroxymethyl group, etc., and n represents 1 or 2], or a pharmacologically acceptable salt or ester thereof, and at least one type of drug selected from an insulin sensitizer, an insulin secretagogue, a biguanide drug, an insulin preparation and a DPP-IV inhibitor.
US7476668 Thiadiazine derivatives and use thereof as positive AMPA receptor modulators Compounds of formula (I): wherein: A represents thienyl, furyl, pyrrolyl, oxathiol, thiazole, isothiazole, oxazole or imidazole, represents a single bond or a double bond, R1 represents hydrogen, linear or branched (C1-C6)alkyl optionally substituted by one or more groups selected from halogen or (C1-C6)alkoxy-(C1-C6)alkyl, R2 represents hydrogen or linear or branched (C1-C6)alkyl group optionally substituted by one or more halogen, R3 represents hydrogen or a group selected from linear or branched (C1-C6)alkyl, CONHR′ and SO2NHR′ wherein R′ represents linear or branched (C1-C6)alkyl, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same, which are useful as AMPA inhibitors.
CN101019865A Compound nicotinamide medicine for antiphlogosis, wet storage and eliminating spot The compound nicotinamide medicine for antiphlogosis, wet storage and eliminating spot consists of nicotinamide 2-10 wt%, trans- or cis-vitamin A acid 0.025-0.05 wt%, and corticosteroid 0.025-1 wt%. It has functions of moistening skin, diminishing inflammation, inhibiting melanogenesis, and treating eczema, skin pruritus, acne, etc.
US20100297266 Preparations and methods for textile and or fiber surface finishing, surface finished articles prepared thereby, and uses therefor Disclosed are food compositions, comprising aqueous extracts of Melissa officinalis (Lemon balm) and/or its active principle rosmarinic acid. Methods of preparing a food composition, and of making a medicament, both methods comprising rosmarinic acid and/or aqueous extracts of Melissa officinalis, are also disclosed.
CN101890082A Medicinal composition for treating depression and manufacturing method thereof The invention discloses a medicinal composition for treating depression, which is prepared by using liquoric root, white paeony root and extracts of the liquoric root and the white paeony root as raw materials. The invention also discloses a preparation method of the medicinal composition. Experiments show that: 1, after 2 days of stomach lavaging, the medicinal composition of the invention can reduce the dead time (P is less than 0.01) and forced swimming accumulated dead time (P is less than 0.05) of a suspended tail of a tested mouse obviously, so it is deduced that the medicinal composition of the invention has experimental depression resistant effect; 2, the combined use of the extracts of the liquoric root and the white paeony root in an optimal ratio achieves an anti-depression effect more advantageous over those obtained by the single use of the liquoric root and white paeony root; and 3, the 5-HT content and NE content of the brain of a chronic stress rat are reduced obviously. The medicinal composition of the invention can improve the 5-HT content and NE content of the brain of the chronic stress rat obviously, which may be one of the mechanisms through which the medicinal composition plays an anti-depression effect.
US20110190237 Macrocyclic Prodrug Compounds Useful as Therapeutics The present invention includes macrocyclic prodrug compounds, pharmaceutical compositions containing them. The present invention also includes use of these compounds in the treatment of various diseases including an autoimmune disease, an inflammatory disease, a neurological or neurodegenerative disease, cancer, a cardiovascular disease, allergy, asthma, a hormone-related disease, and tumors or symptoms resulting from neurofibromatosis.
US20120071425 Uses of mannose-6-phosphate There is provided the use of mannose-6-phosphate, or a salt, precursor or analogue thereof, for providing and/or maintaining a consistent skin colour, particularly to reducing redness of skin. There is also provided the use of mannose-6-phosphate, or a salt, precursor or analogue thereof, as a skin improvement agent for providing a cosmetic effect and mannose-6-phosphate, or a salt, precursor or analogue thereof, for use in treating normal or damaged skin, wherein damaged skin is skin that has been subject to epidermal and/or dermal damage.
US20130022661 Bio-remodable bone augmentation device and method A bio-remodable augmentation device including an implantable member configured for maintaining space in a bone defect. The implantable member is formed from a bio-remodable composite having structural properties so as to aid in the generation of new bone tissue and eventually be reabsorbed in the newly formed bone tissue. This structural and bio-remodable implant reduces, if not eliminates, the need to remove the implantable member from the patient once new bone tissue is formed. A kit including the implantable devices and bone growth material is disclosed. Methods of use are also disclosed.
WO2006111085A1 A method, formulation and use thereor with improved oral absorption of drugs or nutrients A method and composition with altered absorption route of oral drugs and improved total bioavailability, specifically a method, composition and use thereof for absorption of bioactive lipophilic, hydrophilic compounds or mixture of both in gastroenteric system and for improvement in total bioavailability. The special method and composition are characterized in that pharmaceutical or nutritional substances, including monomer compounds and mixture thereof are mixed with one or more organic medium, and mixed with one or more antiacid protector(s). Compositions are manufactured into dosage forms of drugs or nutrients in conventional manner. Clinically, pharmaceutical or nutritional formulations manufactured by process as above are delivered into body orally, resulting in increase in absorption of drugs or nutrients in stomach of a human, decrease in degradation and metabolism of compounds by digestive tract, and improvement in total bioavailability of drugs or nutrients.
CN103055057A Plant weight-losing and fat-reducing composite compatible to L-carnitine The invention provides an L-carnitine combination formula with weight-losing and fat-reducing efficacy and a method for screening the L-carnitine combination formula. A weight-losing and fat-reducing composite which has compatibility effect with L-carnitine is obtained by screening natural products and extracts by taking a triacylglycerol enzyme, amylopsin, fatty acid synthetase, an auxiliary enzyme B as target spots. An optimal composite formula comprises lotus leaves, folium llicis latifoliae, hawthorns, rhizoma alismatis extracts, the L-carnitine, or L-carnitine tartrate and related auxiliary materials. The weight-losing and fat-reducing composite comprises the following components respectively by weight percent (with usage amount in parts by weight): 2%-20%, 1%-15%, 5%-25%, 2%-20%, 20%-85% and 0.5%-10%. The weight-losing and fat-reducing composite provided by the invention is conductive to reducing the redundant fat inside a body and can be used for accelerating the breakdown of the fat inside the body, transforming the fat into energy and inhibiting the absorption of an organism on the fat and saccharide, thereby achieving the purposes of naturally controlling and reducing the weight.
EP2489370A1 Use of a synergistic compound as a therapeutic agent or disinfectant The composition comprises a vitamin, a metal ion, and a surfactant as a therapeutic agent or disinfectant. The quantity of vitamins in the composition is 1-100 mm. The quantity of metal ions is 1-100 mm and the surfactant is 0.1-35 wt.%. The pH value range in the composition is 0.8-8.5.
CN1668287B Use of 3-deoxyflavonoids in preparing medicine for inhibition of t-lymphocyte activation 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-deoxyflavonoid compounds may be increased by administering such compounds along with Rutin, a Rutin congenor and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavonoids may be avoided by administering such compounds by parenteral routes (e.g., sublingual, buccal,intranasal, injection, etc.).
CN101390845A Hard capsule containing etodolac The invention relates to a hard capsule which contains etodolac, the substance in the capsule contains glutin as anti-crosslinking agent; the hard capsule which contains etodolac has the advantages of good stability, avoiding the crosslinking reaction on the capsule shell, being applicable to analgesia, diminishing inflammation and antipyretic.
WO2010133544A1 Piperazine and aminopyrrolidine compounds as histamine h3 receptor antagonists The invention relates to compounds of formula (I) wherein R1 to R3 and X0, X1, X2 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
WO2011016527A1 Hydroxyl radical generator, antiviral material using hydroxyl radical generator, and method for generating hydroxyl radicals Disclosed are: a hydroxyl radical generator which is capable of efficiently generating hydroxyl radicals; an antiviral material using the hydroxyl radical generator; and a method for generating hydroxyl radicals. Specifically disclosed is a hydroxyl radical generator which is composed of a mixture that contains a titanium oxide powder and a powder or solution of an additive that is compose of at least one substance selected from the group consisting of a partial hydrate of dolomite, silver oxide, aluminum hydroxide, aluminum oxide, magnesium hydroxide, calcium hydroxide, potassium hydroxide and sodium hydroxide. The mixture contains 99-1% by weight of the titanium oxide and 1-99% by weight of the additive.
EP1911494A2 Use of oligosaccharides to stimulate beta-endorphin production Use of at least one oligosaccharide comprising 2-6 sugars and containing at least 2 galactose groups, preferably side groups, and especially at the end of the chain, or such oligosaccharide- containing plant extract, as cosmetic or dermatological agent stimulating beta-endorphin production in skin. An independent claim is also included for the process of cosmetic treatment comprising application of at least one oligosaccharide as claimed or such oligosaccharide- containing plant extract, optionally in cosmetically acceptable excipient, onto relevant area of skin.
EP2445491A1 Pharmaceutical composition for emergency contraception The invention relates to pharmaceutical compositions for emergency contraception, to the use of levonorgestrel in combination with cox inhibitors for the production of pharmaceutical compositions for the afore-mentioned purpose, and to a method for producing said pharmaceutical compositions.
CN1907261A Long-acting carbostyril family antibacterial drugs suspension injection The invention discloses a long-effective carbostyrile antibiotic drug injection, which comprises the following parts: 1-10% (W/V) carbostyrile antibiotic medicine, 1-10% (W/V) slow releasing carrier, 15-50% (W/V) alcohol, 1-20% (V/V) surface activator, 10-20% (W/V) water and 50-5% (V/V) and necessary conservative and antioxidant.
WO2012152208A1 Thiazole compound and preparation method and use thereof The present invention disclosed a class of thiazole compounds of general formula (I) and the preparation method and use thereof. More particularly, The present invention disclosed a derivative of natural product largazole, the preparation method thereof and the use in the field of antitumor and multiple sclerosis treatment as a histone deacetylase inhibitor.
CN103505549A Medicine for treating alopecia seborrheica and preparation method thereof The invention provides a medicine for treating alopecia seborrheica and a preparation method thereof. The excessive hair loss caused by pathological factors causes the serious damage to looks, is seriously hurt the self-confidence and also affects the career choice, the marriage and even prospect. The preparation method comprises the following steps: (1) putting 15g of schizonepeta, 8g of radix sileris, 12g of periostracum cicada, 10g of radix rehmanniae, 13g of sophora flavescens, 15g of polygonum multiflorum, 13g of honeysuckle flower, 11g of fructus forsythiae, 10g of dandelion and 10g of liquorice in a marmite, and adding 1kg of water; (2) adding 0.8kg of water again, heating to 100 DEG C, then decocting for 1 hour with slow fire, and filtering out boiling liquid; (3) combing two boiling liquid, when naturally cooling to 40 DEG C-45 DEG C, adding 10mg of vitamin B2, 20mg of vitamin B6 and 50mg of cystine, fully mixing till dissolving; and (4) subpackaging the obtained liquid medicine into two parts. The medicine is used for treating alopecia seborrheica.
WO2011094598A3 Compositions and methods for reversing corticosteroid resistance or treating respiratory infections The present invention features methods for reversing corticosteroid resistance, as well as for the treatment of respiratory infections, particularly those associated with chronic obstructive pulmonary disease. In one embodiment, the method increases Nrf2 biological activity or expression.
EP1928420A1 Treatment of inflammation and vascular abnormalities of the eye Inflammation and vascular abnormalities of the eye, including those related to ischemia, its prophylaxis and its alleviation, are treated by administration to the mammal of small amounts of phosphate-glycerol group presenting bodies such as phosphatidylglycerol liposomes.
EP2616052A1 Methods, compounds and compositions relating to activating a latent virus The present invention relates to, inter alia, an anti-microtubule agent for use in a method of treating a subject having a latent virus, the method comprising: administering the anti-microtubule agent and an anti-viral agent to the subject.
WO2010062686A2 Imidazol-4-one and imidazole-4-thione compounds Imidazol-4-one or imidazole-4-thione compounds of formula (I) shown in the specification. Also disclosed is a method for treating a cannabinoid receptor-mediated disorder with these compounds.
EP1381375B1 Oligonucleotide compositions and their use to induce differentiation of cells The present invention provides compositions comprising a 3'-OH, 5'-OH, chemically unmodified, synthetic phosphodiester nucleotide sequence selected from the group consisting of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, and SEQ ID NO: 4, and a pharmaceutically acceptable carrier, wherein the compositions are useful to induce differentiation of cells or to stimulate differentiation or production of pluripotent cells. The present invention provides methods of using these compositions to induce differentiation of pluripotent cells, including bone marrow derived cells, and to treat disease associated with insufficient differentiation of cells in animals and humans, including but not limited to leukemia, lymphoma, non-malignant blood disorders such as hemoglobinopathies, sickle cell disease, myelodysplastic syndrome, pancytopenia, anemia, thrombocytopenia and leukopenia.
US20110212185 Water that expresses pathogen-resistance genes (pr gene clusters) to encode plant immunoproteins, a method of preventing plant diseases using the water, and a device for producing the water Disclosed is a method of preventing diseases in plants which can bring about a redox reaction in the inside of plant cells thus inducing the expression of pathogen-resistance genes in the plant cells. There is no possibility that residual contents remain in soils. It is also possible to cultivate plants which are strong against diseases. By bringing water which contains reactive oxygen species and allows the reactive oxygen species to be held and to function for a long period into contact with plants, the expression of the pathogen-resistance genes which the plants possess is induced. Accordingly, the water containing reactive oxygen is absorbed into the plants to prevent diseases in plants.
WO2013013609A1 Polymorphic forms of compounds as prolyl hydroxylase inhibitor, and uses thereof The present invention relates to the polymorphic forms of the compound of Formula (I), preparation thereof including the preparation of intermediates and pharmaceutical compositions, and use of a polymorph above in the treatment of a disease, a disorder or a condition, or in the manufacturing of a medicament for the treatment of a disease, a disorder or a condition.
EP1383465B1 Acute pharmacologic augmentation of psychotherapy with d-cycloserine Methods for treating an individual with a psychiatric order with a pharmacologic agent that enhances learning or conditioning in combination with a session of psychotherapy are provided. These methods of the invention encompass a variety of methods of psychotherapy, and psychodynamically oriented psychotherapy, and psychiatric orders including fear and anxiety disorders, addictive disorders, addictive disorders including substance-abuse disorders, and mood disorders. The pharmacologic agents used for the methods of the present invention are ones that generally enhance learning or conditioning, including those that increase the level of norepinephrine in the brain, those that increase the level of acetylcholine in the brain, and those that enhance N-methyl-D-aspartate(NMDA) receptor transmission in the brain.
WO2013051639A1 Pyrazoloquinoline derivative A compound represented by formula (I) or a pharmacologically acceptable salt thereof which has an inhibitory effect on PDE9 and, therefore, is expected as being capable of increasing the cGMP level in the brain. Since the inhibitory effect on PDE9 and an increase in the cGMP level contribute to improvement in learning and memory behavior, the aforesaid compound or a pharmacologically acceptable salt thereof would be available as a remedy for cognitive dysfunction in Alzheimer's disease. In formula (I): R1 represents a hydrogen atom; R2 represents an aromatic ring group, etc.; R3 represents a hydrogen atom, etc.; R4 represents a hydrogen atom; R5 represents an oxepanyl group, etc.; and R6 represents a hydrogen atom.
CN101269187A Medicament composition for treating bladder cancer and preparation method thereof The invention relates to a drug composition for curing bladder cancer. The drug composition is made of radix rehmanniae recen, talc, herba polygoni avicularis, plantain seed, bamboo leaves, alisma orientale, cassia twig, gardenia jasminoides ellis, liquorice, angelica, rhizoma ligustici wallichii, ginseng, white paeony root, dogwood, root-bark of tree peony, tuckahoe and/or a medically acceptable carrier. The invention also relates to a method for preparing the drug composition. The drug composition has the functions for clearing heat and promoting diuresis, promoting blood circulation by removing blood stasis, relieving pain, stanching and purging, etc., and can be used for the symptoms of hematuria and urinaryirritation, etc. caused by the bladder cancer.
CN103596571A Methods for treating insomnia Methods for treating insomnia in humans not suffering from any psychiatric disorders using quetiapine.
CA2381143C Dendrimer-photosensitizer complexes for medical applications A method for enhanced PhotoDynamic Therapy (PDT) treatments by applying dendrimer-photosensitizer complexes to bring multiple phototosensitizer moieties to a treatment site is provided. Photosensitizers are covalently coupled to the peripheral bonding places of dendrimers and are being separated in one or more successive cycles. Tetrapyrroles are the photosensitizers employed. In one embodiment the complex is also bound to an antibody or antibody fragment, which aids in targeting the complex to a desired treatment site. After application, the photosensitizers are released, at the treatment site, from the complexes by either light, chemical, or a combined light/chemical effect. Generally the photosensitizers develop their full photodynamic activity as free molecules after being released from the complex. More than one type of photosensitizer may be bound in the complexes. Release and/or activation may be done in a single step or with repeated steps.
CN102895624A Preparation technology and production method for integrated new formulation of Hou's Black Powder The present invention relates to a preparation technology and a production method for an integrated new formulation of a Hou's Black Powder, wherein the raw materials of active ingredients comprise: 40 parts by weight of chrysanthemum, 10 parts by weight of bighead atractylodes rhizome, 3 parts by weight of asarum herb, 3 parts by weight of poria cocos, 3 parts by weight of oyster, 8 parts by weight of balloonflower root, 10 parts by weight of divaricate saposhnikovia root, 3 parts by weight of ginseng, 3 parts by weight of aluminite, 5 parts by weight of radix scutellariae, 3 parts by weight of Chinese angelica, 3 parts by weight of dried ginger, 3 parts by weight of ligusticum wallichii, and 3 parts by weight of cinnamon twig. The production process of the integrated new formulation of Hou's Black Powder comprises the following steps of: supersonic air-jet crushing, alcohol-water extraction, ultrasonic crushing extraction, water decocting concentration, supersonic spray drying, nanometer grinding, high pressure homogenization, nano particle preparation and the like. According to the invention, the advantages, such as multi-synergism, multi-target, embodied by a nano-carrier coupling technique, are focused to be taken of. After the integrated new formulation of Hou's Black Powder is subjected to scale production, the production cost can be greatly reduced, the quality of products is greatly improved and the targeting property and the sustained and controlled release performance of the medicament are enhanced. The internal and external administration of the integrated new formulation of Hou's Black Powder can be realized simultaneously, and can be respectively taken in four time slices according to midnight-noon ebb-flow and qi and blood flowing rule of a human body. The integrated new formulation of Hou's Black Powder can be further prepared into films and transdermal agents which are respectively stuck to different parts of a human body according to the midnight-noon ebb-flow and qi and blood flowing rule of the human body and can be directly absorbed through skin.
CN101991574A Desloratadine external preparation and preparation method thereof The invention relates to a desloratadine external preparation and a preparation method thereof. The external preparation takes desloratadine as a main drug and is used for treating allergic skin inflammation. The desloratadine external preparation can increase the concentration of free drug in skin local tissues of the part with the allergic skin inflammation of a body through percutaneous absorption, have an effective histamine sensitization antagonism role, better play local antianaphylaxis and anti-inflammation efficacies and reduce adverse reactions. The external formulation does not pass through the gastrointestinal tract, thereby avoiding the first pass effect and reduce the probability of occurrence of adverse reactions. The external preparation can be directly applied at the affected side, and the onset of action is rapid. Furthermore, the dose and the coverage area of the external preparation can be selected according to the area and the severity of the affected site, and the external preparation is convenient to use and convenient to carry.
CA2849872A1 New cyclohexylamine derivatives having .beta.2 adrenergic agonist and m3 muscarinic antagonist activities The present invention relates to novel compounds having ß2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
CN102078315A Application of ampelopsin in preparing medicines for treating obesity The invention discloses application of ampelopsin in preparing medicines for treating obesity, and relates to preparation and application of flavonoids compounds. The ampelopsin is used for preparing medicines or health products for treating the obesity, including oral tablets, capsules, granules, oral solution, sustained-release agents, pills and injection solution for treating the obesity, and pharmaceutically acceptable conventional formulations. The ampelopsin has obvious weight-losing effect on obese mice and overweight mice induced by high-fat diet; after the ampelopsin is poured into stomachs of the obese mice in a dose of 25.0mg/kg for 2 weeks, the abdominal fat is obviously reduced, shoulder fat cells are obviously shrunk, the weight is reduced to be normal, and the mice are generally good in conditions, freely acts and have smooth hairs. The maximum tolerance does of the mice through stomach perfusion can reach 18g/kg.
CN102793678A Method for preparing tween-free docetaxel injection The invention relates to a method for preparing a changed formulation of an antitumor medicine sold on the market, in particular to a method for preparing a tween-free docetaxel injection, and belongs to the technical field of medicines and chemical industry. According to the method, poloxamer 407 is used as a carrier of docetaxel, precursor polymer micelles are prepared by a melting method, a powder injection or an injection is prepared, and a stable and clarified docetaxel polymer micelle solution can be obtained by melting the powder injection in water or diluting the injection before the powder injection and the injection are used, so that the solubility of docetaxel is improved, the in-vivo detention time is prolonged, and the adverse reaction caused by using tween-80 is avoided.
EP1921072A1 1,2,3-Triazole derivatives as cannabinoid-receptor modulators The invention relates to the use of compounds having pharmacological activity towards the so-called cannabonid receptors, and more particularly to some 1,2,3-triazole derivatives of formula (I): to processes of preparation of such compounds and to pharmaceutical compositions comprising them.
EP2709626A1 Method for treatment of advanced solid tumors The present invention relates to the use of Volasertib or a salt thereof or a hydrate thereof in combination with Cisplatin or Carboplatin or a salt thereof or a hydrate thereof for treating patients suffering from advanced and/or metastatic solid tumours.
WO2009012259A1 Pentafluorosulfanyl-substituted piperazinylpiperidine derivatives as chemokine receptor antagonists The present invention relates to pentaf luorosulfanyl substituted compounds that modulate the activity of or bind to chemokine receptors such as CCR5, rendering the compounds useful in the treatment of inflammatory diseases, immune diseases and viral infections.
US7365064 Benzoxazine and benzothiazine derivatives and pharmaceutical compositions containing them The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, to a process for preparing such compounds. More particularly, the present invention relates to novel alkyl carboxylic acids of the general, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, to a process for preparing such compounds. The present invention also relates to processes for the preparation of the compounds of formula (I), novel intermediates, processes for their preparation, their use in the preparation of the above said compounds and their use as antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds
CN101088500A Cold treating medicine for children The cold treating medicine for children consists of main medicine components acetaminophen and psedoephedrine hydrochloride, and supplementary material stevioside, microcrystalline cellulose and low substituted hydroxypropyl cellulose. The medicine has high curative effect on children' s cold.
US6849657 Osteoporosis; increase bone density This invention relates to 8-aza prostanoid analogs which are generally EP4 receptor agonists and are represented by Formula I: wherein Q, B, X, J, Z, A and R1-R6 are as defined, their synthesis and use for treatment of osteoporosis and increasing bone density.
US20120321594 Methods of controlling axon or dendrite development of neuronal cells One aspect of the present invention relates to a method of controlling axon or dendrite development in a neuronal cell population. This method involves providing a neuronal cell population and contacting the neuronal cell population with a modulator of R-type Ca2+ channel expression or activity in controlling the neuronal cell population to induce either axon or dendrite development. Another aspect of the present invention relates to a method of treating neuronal injury in a subject. This method involves selecting a subject with neuronal injury mediated by R-type Ca2+ channel expression or activity and administering to the selected subject an inhibitor of R-type Ca2+ channel expression or activity to induce neuronal axon development under conditions effective to treat the neuronal injury in the subject. Yet another aspect of the present invention relates to a method of screening for agents that modulate R-type Ca2+ channel expression or activity.
WO2011083291A1 Combinations comprising an ant i -inflammatory agent and/or an antibacterial agent and a glycosylamine and their use in medicine The present invention relates to pharmaceutical compositions and kits comprising an anti-inflammatory and/or an antibacterial agent, and a glycosylamine such as β,β-di-glucosylamine. Preferably the anti-inflammatory is a COX inhibitor such as aspirin, ibuprofen, naproxen or a selective COX-2 inhibitor. Alternately, instead or in addition to the glycosylamine, the compositions or kits may comprise precursor(s) of the glycosylamine such as glucose and/ or ammonium salts. The compositions and kits are suitable for use in the treatment or prevention of inflammation, pain, fever, cancer or cardiovascular disorders, and for use in the treatment of wounds. The present invention also relates to uses of glycosylamines or precursors thereof to treat or prevent side effects associated with the administration of anti-inflammatories and/or antibacterial agents.
WO2005032522A1 Topical aerosol foams A stable topical aerosol foam is provided. The foam-forming formulation includes a HFA propellant and an active agent in an emulsion. The emulsion has an oil phase and an aqueous, i.e. water-containing, phase. The active agent may be present in either phase or dispersed in the emulsion. The oil phase may consist at least in part of the HFA propellant. Either or both of the oil phase and the aqueous phase may contain one or more surfactants, emulsifiers, emulsion stabilizers, buffers, and other excipients. In an alternative embodiment, the aqueous phase contains a water-soluble active agent, for example, a local anesthetic, and the oil phase contains a water-insoluble second active agent. The foam is stable on the skin, for example for at least 10 minutes at body temperature, and will disappear into the skin upon rubbing or after prolonged standing. The formulation has the advantage of an inert non-flammable hydrofluorocarbon propellant without requiring the use of additional co-solvents or co-propellants. The composition is administered to the skin or mucous membranes.
US20090142385 Compositions for treating bone defects In certain described embodiments, implantable medical materials comprise a scaffolding material, a liquid organic binder, and entrapped calcium-containing particles. The medical materials can incorporate an osteoinductive factor such as a protein. The scaffolding material can bind the factor. In additional described embodiments, implantable medical materials include an osteoconductive scaffolding material, an incorporated osteoinductive factor, and a biodegradable barrier material effective to delay release of the factor from the scaffolding material. The scaffolding material can bind the factor. Also described a methods for preparing and implanting the described medical materials.
US20110070305 Sustained release pharmaceutical composition containing mebicar The invention relates to a sustained release pharmaceutical composition, containing mebicar, for the treatment of anxiety, depression and other psychiatric and neurological disorders.
US20110245231 Active substance and pharmaceutical composition for treating alcohol dependence, and a method for obtaining and the use of said active substance The invention relates to novel drug substance for the treatment of alcohol dependence, pharmaceutical composition, medicament and method for treatment of dependence on using ethyl alcohol containing beverages. The invention provides a drug substance for treating alcohol dependence in human and warm-blooded animals representing substituted 1H-benzimidazoles of the general formula 1 or pharmaceutically acceptable salts and/or hydrates thereof wherein: W represents S or S═0 group; R1 represents one or more substituent selected from hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, optionally substituted azaheterocyclyl; R2 represents hydrogen or optionally substituted C1-C4 alkyl; R3 and R4 independently represent optionally identical substituents selected from hydrogen or optionally substituted C1-C4 alkyl; R5 represents an alkyl substituent selected from hydrogen, optionally substituted C1-C7 alkyl, optionally substituted aryl, optionally substituted heterocyclyl, C1-C4 alkoxycarbonyl, optionally substituted aminocarbonyl.
US20080051429 Use of 4-amino-piperidines for treating sleep disorders Inverse agonists and antagonists of serotonin receptors are disclosed for use in treating sleep disorders such as insomnia, and specifically sleep maintenance insomnia. The compound increase slow wave sleep, decrease the number of awakenings after sleep onset, and decrease the time awake after sleep onset.
WO2006095858A1 Composition for treating bacterial disease in the oral cavity, liquid agent for washing treatment, liquid agent for hemostasis treatment and method of treating bacterial disease in the oral cavity It is intended to provide a therapeutic method, whereby a pain on a patient and the recurrence of any bacterial disease in the oral cavity can be sufficiently inhibited without depending on the removal of a biological tissue, and so on. This therapeutic method is a lesion-sterilization and tissue-restoration method which comprises a washing step wherein a tooth suffering from a bacterial disease in the oral cavity is washed with a liquid agent for a washing treatment, an administration step wherein a therapeutic composition is administered to the thus washed teeth, and a coating step wherein the opening of the teeth is coated. This therapeutic composition comprises an antibacterial agent having an antibacterial effect on the oral bacteria and a base containing polyethylene glycol 400, polyethylene glycol 600, polyethylene glycol 6000 and propylene glycol.
CN102861133A Method for extracting kavalactones by using subcritical water The invention discloses a method for extracting kavalactones by using subcritical water. The method comprises the steps of grinding the roots of Piper methysticum Forst and then adding into a supercritical extraction kettle, feeding deionized water, dynamically extracting for 30 to 60 min under the conditions that the temperature is 110 to 180 DEG C and the pressure is 0.3 to 2 MPa, adding an extracting solution into a macroporous resin for absorption, gradiently eluting with ethanol solution, concentrating an eluent under reduced pressure, extracting a concentrated solution with ethyl acetate for 2 to 3 times, collecting an ethyl acetate layer for concentration, and drying to obtain a product. With the adoption of the method for production, the method is friendly to environment, industrial operation is easily implemented, the extraction efficiency is high, and the production period is short.
EP1363892B1 Method for the production of a stable pharmaceutical form of paclitaxel The stable pharmaceutical form of the anti-cancer drug containing paclitaxel of the Fig. 1, according to the invention, is characterised in that it is a stable form of the active substance of a large surface, amorphous, possibly with some fine-crystalline additive. According to the invention, the method for production of the stable pharmaceutical form of the anticancer drug consists in dissolution of crystalline paclitaxel in a neutral organic solvent selected from the group comprising acetonitrile, dioxane, ethanol, or a mixture of those solvents, with possible addition of water, providing that the control of individual solvents in the mixture is in the range of 5 % to 95 %, while the content of water is in the range of 0 to 60 %; the resulting solution is possibly filtered, frozen, and solvents are removed by sublimation under reduced pressure, at a low temperature, and thereafter the preparation is possibly distributed into doses in conditions assuring its sterility.
CN102988854A Detoxification cream The invention claims a detoxification cream. The cream comprises the following raw materials in parts by weight: 3-5 parts of rhizoma kaempferiae, 0.1-0.4 part of chalcanthite, 2-4 parts of ricepaperplant pith, 6-9 parts of coptis chinensis, 4-7 parts of nux prinsepiae, 0.2-0.6 part of rhizoma alismatis, 3-5 parts of cortex lycii radicis, 2-6 parts of common yam rhizome, 1-4 parts of furnace soil, 2-3 parts of radix clematidis and 2-6 parts of sedum sarmentosum. The detoxification cream not only has the capabilities of clearing heat and drying dampness, purging fire and removing toxin, diminishing swelling and smoothing dieresis, but also has the functions of nourishing the liver and improving the visual acuity, dispelling wind and reducing heat, resisting bacteria and disinfecting; and no side effects are brought to liver, gallbladder, kidney and stomach.
CN101028240B Micro-emulsion/submicro-emulsion in-situ gel preparation for eyes and its making method An in-situ microemulsion / sub-microemulsion gel for treating eye disease is prepared from VA or its derivative, VE or its derivative, oil phase, emulsifier, thickening agent, isotonic regulator, antibacterial agent, pH regulator and purified water through shearing-high-pressure homogenizing process. It has high flowability. If it is dropped in eye, it can become hydrogel.
US7709486 antiviral compounds 1,4,8,11-tetraazacyclotetradecane derivatives for against HIV-infected cells, to inhibit the binding by the natural ligand to its chemokine receptor; viricides The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV- or FIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.
CN1792361A Compound medicine composition for treating hepatitis effectively A composite medicine DDB for treating chronic heptitis B and C features that it contains proportionally diamantane hydrochloride.
US7834030 PPAR agonists; modulate lipid and/or carbohydrate metabolism in mammals; prevention and/or treatment of type-2 diabetes, atherosclerosis, cardiovascular disorders; 3-(2-Chloro-4-{1-[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-yl]-ethoxy}-phenyl)-4H-[1,2,4]oxadiazol-5-one The present invention comprises phenyl-[1,2,4]-oxadiazol-5-one derivatives of the general formula I: wherein the R1-R10 and B, U, V, W, X, Y and Z substituents are defined herein. The claimed invention also comprises the compounds isomers and their physiologically acceptable salts as well as processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
CN102949402A Celecoxib composition, and preparation method and use thereof The invention provides a celecoxib composition. The celecoxib composition contains one or more types of dose units which can be orally released, and each of the dose units contains 50-500mg of celecoxib D95 particles and one or more types of mixtures of pharmaceutical excipients. The composition can be used for treating or preventing diseases caused by COX-2.
US20100249126 Pyrimidine derivatives used as pi-3-kinase inhibitors Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.
CN101278903A Sustained-release injection containing amikacin The invention relates to a slow-released injection comprising amikacin, which comprises a slow-released microsphere and a dissolvent; the slow-released microsphere comprises a slow-release adjuvant and the aminoglycoside antibiotic; the dissolvent is the special dissolvent which comprises a suspending agent such as sodium carboxymethylcellulose, etc., and the viscosity of which is 100cp-3000cp (at 20 DEG C-30 DEC C); the slow-release adjuvant can be selected from EVAc, polifeprosan, PLA, PLGA, sebacic acid copolymer, albumen glue and gelatin, etc.; the slow-released microsphere also can be made into a slow-released implant and an ointment. The slow-released implant and the slow-released injection can be partially placed or injected in a bacterial focus to release locally and slowly for more than 5-30 days, thereby obviously reducing the toxicity of the entire body while getting and maintaining a valid medicine density in the local focus effectively. The slow-released injection comprising the amikacin of the invention has obvious special treatment effect for focus of local infection such as chronic osteomyelitis, severe bedsore, refractory skin ulcer, diabetic foot, osteonecrosis of femoral head and various abscesses ,etc. caused by staphylococcus, streptococcus, peptostreptococcus, propionibacterium acnes, enterobacter, tubercle bacillus, gonococcus and meningococcus, etc.
US20080287483 Polyketides and Their Synthesis and Use The rapamycin gene cluster is an example of a gene cluster which includes a gene (rapL) leading to the formation of a precursor compound (pipecolic acid, in this case) which is required for inclusion in the larger product (rapamycin) produced by the enzymes encoded by the cluster. We have produced a mutant strain containing a rapamycin gene cluster in which the rapL gene is disabled. The strain does not naturally produce rapamycin but does so if fed with pipecolic acid. By feeding with alternative carboxylic acids we have produced variants of rapamycins. Tests have shown biological activity.
WO2014033497A1 5-azaindole compounds with anticancer and antiangiogenic activities The present invention relates to 5-azaindole type compounds responding to the following formula (I): for their use as drugs, and more particularly for the prevention and/or the treatment of diseases and/or disorders chosen amongst cancers; angiogenesis related disorders; parasitic diseases; fungal diseases; autoimmune diseases; inflammatory diseases; warts such as warts caused by papilloma virus. The invention also relates to pharmaceutical compositions comprising such compounds of formula (I). The use of at least one compound of formula (I) as research tool for the cell-cycle synchronization of microtubule drugs resistant cell lines is also part of the invention. Finally, the invention also concerns the use of at least one compound of formula (I) as an herbicide and/or an algaecide.
US20070270431 Preventive and/or Therapeutic Medicine for Rheumatoid Arthritis The present invention relates to a preventive and/or therapeutic medicine for rheumatoid arthritis containing 2-benzyl-5-(4-chlorophenyl-6-[4-(methylthio)phenyl]-2H-pyridazin-3-one and methotrexate. The medicine of the present invention can be administered orally and exhibits suppressed side effects and excellent potency for suppression of arthritis.
CN101402573B Bihydroxyl-2-acyl benzene acetic acid ester, producing method and uses thereof The invention provides a dihydric-2-acyl phenylacetate with a novel structure, a preparation method and application thereof, and relates to a compound containing the structure of the dihydric-2-acyl phenylacetate. The preparation method comprises the following steps: using dihydroxybenzoic acid 1 as a raw material, esterifying the dihydroxybenzoic acid 1, protecting hydroxyl group, reducing estergroup to alcohol 4, and then treating the alcohol 4 by methylsulfonyl chloride and potassium cyanide in turn, obtaining cyanide 6, and then obtaining corresponding phenylacetate 8 by the action of alcohol and the cyanide 6 after the cyanide 6 is hydrolyzed into carboxylic acid; and obtaining an acidylation product (9) by the reaction of the phenylacetate 8 and R<2>CO2H under the action of trifluoroacetic anhydride or polyphosphoric acid, and finally removing the protected group to obtain the dihydric-2-acyl-phenylacetate CsA. Moreover, the dihydric-2-acyl-phenylacetate CsA can also be prepared by adopting an ester exchange method under acid catalysis. The related preparation method has the characteristics of easily obtained reagent, simple operation, high yield, and the like.
CA2301009C Skin care compositions and use The invention provides compositions containing dermaphile oils and methods for their use. Preferred composition contain Purcellin Oil and are useful in treating a wide variety of adverse skin conditions, including disorders manifesting inflammatory and non-inflammatory symptoms and having a variety of etiologies. The compositions are especially useful in treating psoriasis, eczema, acne, surgical scars and sunburn, but are also useful in treating cuts, insect bites, pruritis, cold sores and dry skin. Methods for the use of these compositions are also provided.
WO1999012552A8 9a-AZALIDES AS VETERINARY ANTIMICROBIAL AGENTS 9a-Azalides are useful in the treatment and prevention of bacterial respiratory and enteric infections in livestock animals, particularly in cattle and swine.
WO2007106862A3 The use of statins to stimulate neurogenesis The present invention provides methods of treating a neurogenesis associated condition, e.g. depression or disorders of cognition, comprising administering to a patient in need thereof a therapeutically effective amount of a statin or a pharmaceutically acceptable salt, hydrate, solvate, or pro-drug thereof. These neurogenesis conditions include, but are not limited to, depression, bipolar disorder, schizophrenia, traumatic brain injury, cognitive dysfunction, memory loss, learning disorders, mild cognitive impairment, spinal cord injury, stroke, Alzheimer's disease, Parkinson's disease, Huntington Disease and multiple sclerosis.
CN102229566A Structure of drug for treating neurodegenerative disease The invention discloses a drug structure as shown in the general formula (1), wherein, R1-R5 is independently selected from H, OH, halogen, NO2 or OR, R represents C1-C6 alkyl. The in vitro experiments of pharmacodynamics show that the compound can protect neurons, control Alzheimer disease, and the compound has obvious inhibiting effects to parkinsonism and other neurodegenerative diseases.
WO2012038590A1 Improved dietary substitution for treating or preventing cancer The present invention relates to improved bio-immunotherapy of cancer, especially prostate, breast or cervix cancer. The invention provides an improved dietary supplement composition comprising rubidium in combination with other trace elements, amino acids, vitamins, and neurogenic lipids.
CN1565469A Cornel extract oral medicine compositions low irritative to gastrointestinal tract and its preparation The invention relates to a cornel extract oral medicine compositions low irritative to gastrointestinal tract and its preparation, the oral pharmaceutical composition and preparation of its active constitution, the invention also relates to the process for preparing the oral pharmaceutical composition and preparation.
WO2007011293A1 Novel piperidine derivatives The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.
WO2010084201A1 Novel derivative of erythromycin for the treatment and diagnosis of prion disease The present invention concerns a pharmaceutical composition comprising the (E)-9-[O-(methyl 2-O-benzyl-4,6-O-benzylidene-β-D-allopyranosid-3-yl)oxime] erythromycin A of formula (I) or pharmaceutically acceptable salts thereof, and a pharmaceutically carrier, excipient or diluent; a method of prophylactically and/or therapeutically treating amyloϊd neurodegenerative diseases by administering to a subject in need thereof an effective amount of said pharmaceutical composition; a method for testing at least one sample obtained from a mammal, for the presence or absence of an aberrant prion protein (PrPres) in order to diagnose a Prion infection within said mammal, said method using (E)-9-[0-(methyl 2-O-benzyl-4,6-O-benzylidene-β-D-allopyranosid-3-yl)oxime] erythromycin A; and a kit for detecting the presence or absence of an aberrant prion protein PrPres, the kit comprising at least the (E)-9-[0-(methyl 2-O-benzyl-4,6-O-benzylidene-β-D-allopyranosid-3-yl)oxime] erythromycin A.
WO2013130049A1 Method for enhancing efficacy and selectivity of cancer cell killing by dna damaging agents The invention relates to the treatment of cancer using DNA damaging agents. The invention provides methods for treating a mammal with cancer, the method comprising inhibiting in the mammal acidic residue methyltransferase (Arm1) in combination with administering to the mammal a DNA damaging agent. The invention further provides pharmaceutical formulations comprising an inhibitor of acidic residue methyltransferase (Arm1) and a DNA damaging agent.
WO2008016890A1 Antitumorigenic drug combination Compositions for treating cancer, in particular non-Hodgkin' s lymphomas, in a mammal comprising therapeutically effective amounts of an antimitotic agent and a peptidomimetic of the second of the three Type-1 repeats of thrombospondin-1 (TSP-1) or a salt of either or both.
CN101531697A Method for preparing sarsasapogenin in rhizoma anemarrhenae and derivatives thereof, and novel pharmaceutical application of the sarsasapogenin in the rhizoma anemarrhenae and the derivatives thereof The invention belongs to the technical field of medicaments, relates to a method for preparing high-purity sarsasapogenin in rhizoma anemarrhenae and derivatives thereof, and also relates to novel pharmaceutical application of the derivatives of the sarsasapogenin. The method comprises the following steps that: a rhizoma anemarrhenae medicinal material is extracted by aqueous ethanol or/and water; a macroporous absorbent resin is adopted for adsorption and elution; the acid hydrolysis and the recrystallization are performed; and the purity of the prepared high-purity sarsasapogenin reaches 98 percent. Compared with the prior art, the method has the advantages of low cost, low content of product impurities, stable preparation technology, easy operation, easy realization, and no pollution to the environment during the production. The method also synthesizes a series of the derivatives of the sarsasapogenin through a chemical synthesis method, and a pharmacological experiment proves that the derivatives of the sarsasapogenin have antiaging activity. The pharmaceutical application of the sarsasapogenin and the derivatives thereof in preparing medicaments for anti-senile dementia, antiaging and antidepressant is developed through the pharmacological activities of the sarsasapogenin and the derivatives thereof.
US20120171303 Compositions and methods for ehnancing cognitive and related functions in animals Compositions comprising melatonin and one or more carotenoids and methods for using such compositions for enhancing cognitive and related functions such as reducing or preventing a decline of social interaction, reducing or preventing age-related behavioral changes, increasing trainability, improving attention, maintaining optimal brain function, facilitating learning and memory, reducing memory loss, and preventing or treating cognitive decline caused by dementia in an animal. Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.
US6908922 Linear cyclic ureas Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i), (ii) or (iii): Medicinal products containing the same which are useful in the treatment of diseases or pathological conditions ins which endothelial dysfunction is known.
CN103705506A Application of enilconazole in preparing drug for treating or preventing influenza virus infections The invention discloses an application of enilconazole in preparing a drug for treating or preventing influenza virus infections. Firstly, toxicity of enilconazole to MDCK cells is detected. The result shows that the maximum non-toxic concentration of enilconazole is 100.0 [mu]M. Secondly, antiviral activity of enilconazole is measured within a completely non-toxic concentration range. The result shows that the small molecular compound has significant antiviral activity and the antiviral activity presents a dosage-dependent effect. Finally, the antiviral activities of enilconazole to influenza viruses in different types and subtypes are detected. The results show that enilconazole can suppress replication of all the detected influenza virus strains in a dose-dependent manner, so that the anti-influenza virus activity of enilconazole has a broad spectrum. Therefore, enilconazole disclosed by the invention is a novel broad-spectrum anti-influenza virus drug and can be used for preparing the drug for treating or preventing the influenza virus infections.
EP2782917A1 Thienopyrimidine inhibitors of atypical protein kinase c The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have a PKC inhibitory activity, and may be used to treat proliferative disorders.
CN103520726A Preparation method of invisible thermosensitive liposome as well as application of drug delivery system of invisible thermosensitive liposome in tumor treatment drugs The invention relates to a preparation method of a drug delivery system of an invisible thermosensitive liposome as well as an application of the drug delivery system of the invisible thermosensitive liposome in tumor treatment drugs, and can be used for effectively solving the problems that an existing tumor treatment drug is large in side effect, poor in treatment effect, and the like. The drug delivery system of the invisible thermosensitive liposome is composed of a thermosensitive liposome-loaded targeted heat sensitizing agent and chemotherapy drugs in a weight ratio of 1:3, wherein the invisible thermosensitive liposome is obtained through synthesis of carboxylic nanotubes, synthesis of folate-targeted carbon nano tube-lysine, preparation of the invisible thermosensitive liposome or synthesis of carboxylic nanotubes, synthesis of carbon nano tubes loaded with chemotherapy drugs, and preparation of the thermosensitive liposome. The preparation method disclosed by the invention is good in physical and chemical stability, simple and practicable in preparation condition, rich in material resources, low in cost, small in side effect and capable of effectively restraining multiplication of tumor cells, so that the effect of tumor-targeted treatment is achieved, and therefore, the preparation method is an innovation of a drug carrier in tumor-targeted treatment.
WO2011105590A1 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor Disclosed is a novel 1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine derivative, a pharmaceutically acceptable salt thereof or a solvate thereof, which is useful as an anti-HIV agent. Specifically disclosed is a compound represented by general formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof. (In the formula, the symbols are as defined in the description.)
US7109323 lyophilization of an aqueous mixture comprising a boronic add compound and a compound having at least two hydroxyl groups produces a stable composition that readily releases the boronic acid compound upon dissolution in aqueous media The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic acid compounds and methods for preparing the compositions. The invention also provides novel boronate ester compounds. The invention further provides boronic acid anhydride compounds useful in the methods of the invention.
US8063083 Method for treating non-Hodgkin's lymphoma The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating non-Hodgkin's lymphoma, in a subject in need thereof.
CN101810603A Aerosol taking salbutamol and ambroxol as active ingredients The invention relates to an aerosol taking salbutamol and ambroxol as active ingredients, which is prepared from salbutamol and ambroxol or salts thereof, or purified hydrates thereof serving as medicinal active ingredients and pharmaceutically acceptable auxiliary materials. The aerosol is prepared by adding some specific types of auxiliary materials in certain proportions and blowing a certain amount of propellent into the salbutamol and ambroxol or the salts thereof, or the purified hydrates thereof serving as raw materials according to the technological measure stated by the invention, and is used for suction.
US20090149501 administering [7-(benzyloxy)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-indol-3-yl](2,2,3,3-tetramethylcyclopropyl)methanone to mammals as analgesics, antiinflammatory agents and as neuroprotectants The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.
US8841310 Combinations of a pyrimidine containing NNRTI with RT inhibitors The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.
US20090304648 Mast Cell Stabilizers to Prevent or Treat Laminitis Provided herein are mast cell stabilizers used to prevent, treat, or mitigate severity of laminitis. Mast cell stabilizers can be combined with antihistamines and other medicaments to prevent, treat, or mitigate severity of laminitis.
WO2010094009A3 Methods and compositions for the treatment of ras associated disorders The instant disclosure relates to compositions that may be useful as therapeutic agents for the treatment of disorders associated or caused by Ras deregulation or dysregulation, for example, disorders associated with alterations in the NFl gene such as neurofibromatosis type I and/or fungal infections such as those caused by Candida albicans.
WO2009044899A1 Nucleic acid capable of regulating the proliferation of cell Disclosed are: an agent for inhibiting or promoting the proliferation of a cell; a diagnostic or therapeutic agent for a disease associated with the abnormal proliferation of a cell; an apoptosis inducer; an agent for inhibiting or promoting the expression of a target gene of a nucleic acid, such as microRNA; and a method for inhibiting or promoting the proliferation of a cell.
CN101214237B Pharmaceutical use of dandelion xylogen acid for inhibiting acetylcholine esterase The present invention relates to lignin acid which is obtained by being separated from taraxacum plant and the strong activity of the compound of inhibiting acetylcholinesterase. Mongolian taraxacum acid A is prepared by being separated and purified from the taraxacum, which is 6, 9, 10-trihydroxy- xanthene-1, 2-dicarboxylic acid that has obvious inhibiting effect towards the acetylcholinesterase, therefore the compound, officinal salt thereof and medicine combination which is made from the medicine excipient or the carrier allowed by the preparation can be expected with a purpose of being used as a drug for remedying the senile dementia.
CN101590064A Anti-infection skin sterilizing agent for external use The invention relates to a prescription and a preparation method of a broad-spectrum sterilizing and anti-infection sterilizing agent, which can be widely used for the sterilization and the anti-infection of various skin body surfaces. The invention has the advantages of being widely used for the sterilization and the anti-infection of various skin body surfaces, good sterilizing effect, no damage on sterilized articles, safety, no toxicity, no environmental pollution, good product performance, low cost, convenient use and wide popularization and application.
WO2011147175A1 PREPARATION OF MICROVESICLE-siRNA COMPLEXES AND USE THEREOF IN AIDS TREATMENT Drugs for AIDS treatment are provided, which comprises microvesicles carrying specific anti-HIV siRNAs. Methods for preparing said drugs are also provided.
US20100210695 Compositions and methods for treating skin disorders The present invention is directed to pharmaceutical compositions formulated for topical administration comprising an inhibitor of carnitine palmitoyl transferase (CPT1) and methods for treating skin disorders, such as psoriasis, by administration of a CPT1 inhibitor. In particular embodiments, the invention provides a pharmaceutical composition formulated for topical administration comprising the CPT1 inhibitor ST1326. In other embodiments, the invention provides a method of treating a skin disorder, such as psoriasis by administration of the CPT1 inhibitor ST1326.
US20100292205 Pyrimidone Compounds As GSK-3 Inhibitors The invention pertains to pyrimidone compounds that serve as effective GSK-3 inhibitors. The invention further relates to pharmaceutical compositions and methods comprising such pyrimidone compounds; and the use of such compounds for treating certain disorders.
US20120034278 Ophthalmic preparation containing menthyl ester of indomethacin There is provided an ophthalmic pharmaceutical preparation comprising menthyl ester of indomethacin as an active ingredient. Also provided are different possible formulations of the ophthalmic preparation, and different methods of treating ophthalmic irritation using the ophthalmic preparation.
US20080009531 5-Anilino-4-Heteroarylpyrazole Derivatives Useful for the Treatment of Diabetes The present invention relates to 5-anilino-4-heteroarylpyrazole compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.
WO2006038802A1 Stabilised oxygen releasing composition The present invention relates to stabilised liquid oxygen releasing composition comprising a component (a) selected from the salts consisting of cations An+ and anions derived from halogen oxides according to the general formula [OmX]- wherein A is a metal selected from Groups 1 or 2 of the Periodic System of the Elements, X is a halogen atom, m = 1 - 4, n = 1 or 2, a component (b) selected from the group of oxygen donors, a component (c) selected from the group of oxygen donor stabilising agents and a component (d) selected from the group of liquid binders. The stabilised liquid oxygen releasing composition can be used in pharmaceutical compositions, cosmetic compositions and food applications, e.g. skin care products, dental care products, tooth whitening products including chewing gums.
EP0934281B1 1-phenyl-benzimidazole compounds and their use as baga- a? receptor modulators The present invention relates to novel benzimidazole compounds, represented by general formula (I) in which o is 0, 1, 2, or 3; R1 represents an alkyl group, a phenyl group, or a monocyclic heterocyclic group, which groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkyl-alkyl, alkoxy, halogen, trifluoromethyl, cyano, amino, and nitro; or R1 represents a cyano group or a group of the formula -alkyl-CO¿2R?2, alkenyl-CO¿2?R?2, -CO-R2, -CO¿2(CH2)mR2, or -C(R?3)=N-OR2, R11¿ represents a group of formula -CO¿2?-R?9, or R11¿ represents a group of general formula (II) in which n is 0, 1, 2 or 3; or R11 may represent a group of general formula (III), in which n is 0, 1, 2, or 3; the novel compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABA¿A? receptor complex, such as for example anxiety, sleep disorders, anaestesia, memory disorders, and epilepsia or other convulsive disorders.
WO2005007845A3 Transgenic cells We describe transgenic cells comprising nucleic acid molecules that comprise nucleic acid sequences which encode enzymes involved in the biosynthesis of n-3 fatty acids.
CN103284943A Novel method for preparing penehyclidine hydrochloride injection The invention discloses a novel method for preparing a penehyclidine hydrochloride injection and belongs to the field of medical drugs. The preparation process of the injection comprises the following steps: (1) performing acid treatment on an inner package in advance, washing with pure water and water for injection, performing high-temperature sterilization and drying for later use; (2) weighing penehyclidine hydrochloride according to the prescription amount, adding a proper amount of water for injection for dissolving, regulating the pH of the liquid medicine to be 4.6-4.8 by using a pH regulator, adding the water for injection to the total amount, and uniformly stirring; (3) measuring the pH value and the content, filtering and encapsulating the water in the spare inner package after the water is qualified, and sterilizing at a high temperature to obtain the injection. The penehyclidine hydrochloride injection product prepared by the process method is stable in pH and content, and the product quality is easily guaranteed; meanwhile, the long-term animal toxicity test and pharmacodynamic test prove that the final product is safe and effective.
CN102973555A Pharmaceutical composition containing Ftibamzone compound and preparation method thereof The invention relates to a pharmaceutical composition containing Ftibamzone compound and a preparation method thereof. The pharmaceutical composition containing the Ftibamzone compound is prepared by a formulation consisting of the following components in percentage by weight: 2.5-3.5% of the Ftibamzone, 0.05-0.1% of tretinoin, 8.0-10.0% of mixture of hexadecyl alcohol and stearyl alcohol, 4.0-6.0% of liquid paraffin, 6.5-7.5% of glycerin monostearate, 0.5-1.5% of Twain-80, 0.15-0.25% of ethyl p-hydroxybenzoate, 10.2-12.2% of propylene glycol, 0.5-1.5% of lauryl sodium sulfate, 56.5-58.6% of purified water, 4.0-6.0% of dimethyl sulfoxide, 56.94% of the purified water and 4.0-6.0% of the dimethyl sulfoxide. The pharmaceutical composition, provided by the invention, is mainly used for treating plane warts, can reduce scars caused in treatment, and is simple in preparation process, good in stability, remarkable in treating effect and convenient to use.
EP1385837B1 Tricyclic alkylhydroxamates, their preparation and their use as cell proliferation inhibitors Compounds of formula (I), wherein R1, R2, A, X, Y and Z have the meanings defined in the specification, process of manufacturing these compounds and pharmaceuticals with HDAC inhibitor activity containing such a compound.
US20100080859 Method for attenuating free radical formation resulting from a bodily insult A method is provided for attenuating free radical formation resulting from a bodily insult. The method includes administering bicarbonate to the body of a subject at a dosage ranging from 1.5 mEq/kg of body weight to 5.0 mEq/kg of body weight within a 24-hour period.
CN103156871A Method of avoiding phenomenon of accelerating blood clearance by continuously and repeatedly injecting polyethylene glycol (PEG) lipidosome of epirubicin hydrochloride The invention belongs to the field of medical technology, relates to a method of avoiding a phenomenon of accelerating blood clearance by continuously and repeatedly injecting polyethylene glycol (PEG) lipidosome of epirubicin hydrochloride, and particularly relates to the influences of the pharmacokinetics behavior of the epirubicin hydrochloride in the second injection of the PEG epirubicin hydrochloride lipidosome by the first injection of blank lipidosome and PEG epirubicin hydrochloride lipidosome and the phenomenon of accelerating blood clearance by continuously and repeatedly injecting the PEG lipidosome. Dosage of PEG epirubicin hydrochloride lipidosome is provided to relieve or avoid the acceleration of the blood clearance on the mentioned basis. By changing the dosage of the epirubicin hydrochloride of the first injection or the continuous injection, the method reaches the purpose of preventing drugs from releasing from the lipidosome and relieving or eliminating the acceleration of the blood clearance.
EP2189440A1 Tricyclic amine compound A compound represented by the following general formula (I): [wherein R1 represents hydrogen atom or a C16 alkyl group, A and B represent -(CH2)2-, -(CH2)3- or -(CH2)4-, X represents -N(R2)- (R2 represents hydrogen atom or a C1-6 alkyl group), -CO-, -C(=N-R3)- (R3 represents hydrogen atom or a C1-6 alkyl group), or - C(=C(R4)(R5))- (R4 and R5 independently represent hydrogen atom or a C1-6 alkyl group), and Ar represents an aryldiyl group or a heteroaryldiyl group], which has an action of controlling physiological activities of retinoids and useful as an active ingredient of a medicament.
US7928143 Method for preventing and/or treating neurodegenerative diseases The invention relates to a neurodegenerative disease treating agent for parenteral use, which comprises (2R)-2-propyloctanoic acid or a salt thereof. Since the neurodegenerative disease treating agent of the present invention comprising (2R)-2-propyloctanoic acid or a salt thereof, characterized in that a dosage exceeding about 100 mg per dose is parenterally administered, shows neuropathy improving effect and S-100β increase inhibiting effect in patients with cerebral infarction, it is useful for the treatment of neurodegenerative diseases including cerebral infarction. In addition, it is also useful as a neural regeneration agent after transplantation.
EP2441456A1 DHEA compositions for treating menopose A sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone-sulfate, androst-5-ene-3β,17β-diol, and 4-androsten-3,17-dione for use in a method of treating and/or reducing the likelihood of acquiring symptoms or diseases due to the menopause, or vaginal diseases or problems, in postmenopausal women is provided, said method comprising administering the sex steroid precursor to a patient in need of said treatment at a therapeutic amount which increases the level of circulating androgen metabolites, as part of a combination therapy with a therapeutically effective amount of a Selective Estrogen Receptor Modulator in order to decrease the risk of breast and uterine cancer normally present in postmenopausal women and to prevent bone loss, fat accumulation and diabetes type 2. Pharmaceutical compositions and kits for delivery of active ingredients useful to the invention are disclosed.
EP1509538A1 6,11 bicyclic erythromycin derivatives The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
US20080103109 Distributing polynucleotide in vivo using conditional vector that is transcriptionally active in normal cells and not in malfunctioning cells The invention generally relates to targeted gene therapy using recombinant vectors and particularly adenovirus vectors. The invention specifically relates to replication-conditional vectors and methods for using them. Such vectors are able to selectively replicate in a target tissue to provide a therapeutic benefit from the presence of the vector per se or from heterologous gene products expressed from the vector and distributed throughout the tissue. In such vectors, a gene essential for replication is placed under the control of a heterologous tissue-specific transcriptional regulatory sequence. Thus, replication is conditioned on the presence of a factor(s) that induces transcription or the absence of a factor(s) that inhibits transcription of the gene by means of the transcriptional regulatory sequence with this vector; therefore, a target tissue can be selectively treated.
US6858620 For therapy of male erectile dysfunction; female arousal disorder Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosed
WO2013058194A1 Srf signal activating agent Provided are a pharmaceutical product, a quasi-pharmaceutical product, a food, an animal food, and a material mixable thereto that have an excellent SRF signal activation effect and are highly safe. This SRF signal activating agent comprises, as an active ingredient, at least one type of ingredient selected from juniper berry extract, yucca extract, basil extract, mustard oil, purple corn colorant, tocopherols, and chlorophyll.
CN103338746A Composition containing polyunsaturated fatty acid The purpose of the present invention is to provide a composition for external applications, in which the long-term stability of a polyunsaturated fatty acid is further increased. The present invention provides a composition as mentioned below. In the composition, the long-term stability of a polyunsaturated fatty acid is improved. A composition comprising components (A) and (B) as mentioned below, wherein the component (B) is dispersed in a continuous phase containing the component (A): (A) at least one component selected from the group consisting of tocopherol and phytic acid; and (B) a liposome containing a polyunsaturated fatty acid or a derivative thereof.
CN101559054B Use of chemical compound medicament for curing alcohol dependence The invention relates to a chemical compound medicament for curing alcohol dependence. The chemical compound medicament is characterized by containing GABAB receptor stimulating agent baclofen bulk medicament, M receptor antagonist paralest bulk medicament and auxiliary material. The material comprises the following effective components by the weight percent: 0.3-15 of baclofen, 0.05-5 of paralest and 80-99.65 of auxiliary material. Taballa or medicament in other forms is prepared by regular methods. The chemical compound medicament has remarkable curative effect and little side effect in the aspects of abstinence, rehabilitation and relapse resistance for alcohol reliers.
US20120128763 Lubricant for the ocular surface A formulation has been developed for treatment of the symptoms of dry eye which incorporates the natural product jojoba wax, or components thereof, to enhance the spreading of the artificial tear and eyedrop as well as stabilize the eyedrop. The improved performance of the jojoba wax supplemented tear relieves irritation and discomfort as well as sharpens the blurred vision.
US20120010235 N-substituted pyrrolidines Compounds of formula and enantiomers and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control, amelioration or prevention of cancer.
US7271192 Nitrogen oxide synthase inhibitors; synthesis Novel 2-pyrrolidin-2-yl-1H-indole compounds corresponding to formula (I) wherein R1, R2, R3 and R4 have the meanings given in the description, and pharmaceutical compositions containing these compounds, as well as processes for the preparation of such compounds and intermediate products of this process, and related methods of treatment.
WO2010142890A1 Composition including a molecule promoting the neuron-glia interaction, in particular for preventing the formation of the glial scar and inducing neural regeneration The invention relates to compositions, in particularly pharmaceutical ones, including at least one arylcyclohexylamine derivative, or at least one pharmaceutically acceptable salt of said derivative, as an active agent modulating the neuron-glia interaction, particularly for inducing neural regeneration, in particular in the chronic treatment of medullar trauma or for limiting or preventing the glial scar or any other astrocyte reaction that could impair neuronal survival or axonal regrowth.
CN101912376B Matrine vaginal effervescent tablets with bilayer structure and preparation method The invention discloses a matrine-containing vaginal effervescent preparation. The preparation comprises an alkaline inner layer and an acidic outer layer, is used for treating vaginal infection of women and gynecological inflammation caused thereby, has a reasonable formula and cannot cause adverse reactions such as vulvovaginal stimulation symptoms and the like. In addition, the invention also relates to a preparation method and application of the preparation in preparation of medicaments for treating diseases such as bacterial vaginosis, candidal vulvovaginitis and/or trichomonas vaginitisand the like.
WO2010139967A1 Dihydroindole and tetrahydroisoquinoline derivatives useful as potassium channel inhibitors A compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein; A represents a chemical moiety with the general formula (II); X and Y are independently selected from a group consisting of CH2, CH(R5) or C(R5)(R6); R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino sulfonyl or nitrile; R4 is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted sulfonyl, optionally substituted sulfamoyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl; R5 and R6 for each occurrence is optionally substituted alkyl; R7 and R8 are the same or different and each represents hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; n = 0, 1, 2 or 3; o = 0, 1 or 2 with the proviso that when o = 0, n is 1, 2 or 3 and when o = 1, n is 1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. These compounds are useful in the treatment of various disorders including arrhythmia.
EP1212298B1 Isolation of natural l-beta-3-indolylalanine and enrichment of natural aliphatic amino acid mixtures with natural l-beta-3-indolylalanine A process for isolating substantially pure natural L-β-3-indolylalanine (L-β-3) from a mixture of amino acids, such as a protein hydrolysate, is described. A protein hydrolysate, for example of casein or soy protein, is passed over a polymeric resin attractive to aromatic amino acids but not attractive to aliphatic amino acids. The aromatic amino acids are retained on the resin while the aliphatic amino acids pass over the resin and are collected. The resin is then washed with water to displace any residual aliphatic acids which may be physically associated with but not bound to the resin. Thereafter, the resin is eluted with a dilute acid to displace L-phenylalanine and L-tyrosine and provide a solution thereof while allowing L-β-3 to be retained on the resin. The resin is then further eluted with a dilute base to displace L-β-3 from the resin and provide a solution of L-β-3. Substantially pure natural L-β-3 is recoverable from this solution.
EP1539734B1 Piperidine quinolyl propyl derivatives and use thereof as antimicrobial agents The invention concerns piperidine quinolyl derivatives of general formula (I)) wherein: R1a is hydrogen, halogen, hydroxy, amino, alkylamino, dialkylamino, hydroxyamino, alkyloxyamino or alkyl alkyloxy amino and R1b is hydrogen, or R1a and R1b form an oxo; R2 is carboxy, carboxymethyl or hydroxymethyl; R3 is alkyl substituted either by phenylthio optionally substituted by halogen, hydroxy, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxy, alkyloxycarbonyl, cyano or amino, or by cycloalkylthio (3 to 7 members) optionally substituted by halogen or trifluoromethyl, or by heteroarylthio (5 to 6 members and 1 to 4 heteroatoms selected among N, O and S), optionally substituted par halogen, hydroxy, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxy, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl, or heteroaryl such as defined above; R4 is alkyl, alkenyl-CH2- or alkynyl-CH2-, cycloalkyl or cycloalkyl alkyl, in their various separated or mixed isomeric forms, as well as their salts. Said novel derivatives are potent antibacterial agents
CN102218083A Drug composition for treating and preventing ophthalmic diseases The invention provides a formula for rapidly and effectively treating and preventing ophthalmic diseases, and a preparation method; the formula is a drug composition comprising lutein, taurine, and organic trace elements; the cell oxygen supply effect of organic germanium is especially emphasized, and is the base of quicker clinical curative effect; and the formula has the characteristics of quick results and consolidated efficacy on relieving ophthalmic diseases such as eye fatigue, myopia, fundus damage, etc. The components of the formula comprises: lutein, yeast zinc, yeast selenium, yeast chromium, organic germanium and taurine. In clinical observation of volunteers, the drug composition is proved to have the efficacy of rapidly relieving eye fatigue, rapidly improving blurred vision, eliminating muscae volitantes, and effectively controlling cataract and diabetic retinopathy, and is a drug composition with broad market in the ophthalmology field.
US20080167312 Preparation and utility of substituted allylamines Disclosed herein are substituted allylamines having structural Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and the methods of their use thereof.
US20090149542 Administering 2-hydroxy-5-(2-(4-trifluoromethyl-phenyl)ethylamino)-benzoic acid The present invention relates to 2-hydroxy-alkylamino-benzoic acid derivatives and to a combination of cell necrosis inhibitor and lithium, process for the preparation of the derivatives or the combination, pharmaceutical formulation containing the derivatives or the combination, and use of the derivatives or the combination by either concomitant or sequential administration for improvement of treatment of neuronal death or neurological dysfunction. The derivatives and the combination of the present invention are useful for treating neurological diseases, such as amyotrophic lateral sclerosis (ALS, Lou Gehrig's disease), spinal muscular atrophy, Alzheimer's disease, Parkinson's disease, Huntington's disease, stroke, traumatic brain injury or spinal cord injury; and for treating ocular diseases such as glaucoma, diabetic retinopathy or macular degeneration.
WO2012003190A1 Riminophenazines with 2-(heteroaryl)amino substituents and their anti-microbial activity The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
EP1615630A1 Method for the treatment of diseases linked to an accumulation of triglycerides and cholesterol The present invention concerns a method for the treatment and/or the prevention of diseases linked to the accumulation of triglycerides in tissues and blood comprising at least the step of administering to a human or non human animal in need thereof, as therapeutically active agent, an effective amount of (3-aminoisobutyric acid, derivative, prodrug, metabolite or complex thereof.
CA2339792C Opthalmic solution with tetracycline for topical treatment of dry eye disease Ophthalmic compositions and methods of using the same to simultaneously treat eye surface inflammation and dry eye are disclosed. The ophthalmic preparation contains a tetracycline compound in aqueous solution,. The preparation preferably further includes a balance of electrolytes sufficient to maintain or restore essentially normal levels of conjunctival mucus-containing goblet cells and corneal glycogen. These electrolytes can include potassium, chloride, bicarbonate, sodium, calcium, magnesium and phosphate.
WO2013056015A1 Isoindolinone and pyrrolopyridinone derivatives as akt inhibitors The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.
CN101371838A Novel uses of neferine and analogue thereof The invention discloses the new application of neferine and a neferine analogue. The invention refers to the application of the neferine, as shown in a formula (I), and the neferine analogue or a pharmaceutically acceptable salt of the neferine in the preparation of a medicament for inhibiting the proliferation of eukaryotic tumor cells and a medicament for preventing and/or curing a tumor. The neferine and the neferine analogue or the pharmaceutically acceptable salt shown in the formula (I) can combine with G-quadruplex DNA to increase the stability of the G-quadruplex DNA, thereby competitively inhibiting the combination of telomerase and telomere and the activity of the telomerase, weakening the proliferation ability of a cell, controlling the extension of the telomere and accelerating the apoptosis of the cell. That the neferine and the neferine analogue or the pharmaceutically acceptable salt shown in the formula (I) is used for preparing the medicament for preventing and/or curing the tumor has great meaning.
CA2200991C Compounds for the suppression of hiv tat transactivation The present invention reveals the isolation, purification and characterization from the creosote bush Larrea tridentata of compounds of structural formula (I) where R1, R2, R3 and R4 are each selected from the group consisting of HO-, CH3O- and CH3(C=O)O-, provided that R1, R2, R3 and R4 are not each HO- simultaneously. Each compound is a derivative of 1,4-bis-(3,4-dihydroxyphenyl)-2, 3--dimethylbutane (nordihydroquaiaretic acid, NDGA). In addition, NDGA and each derivative can be used in a method to suppress Tat transactivation of a lentivirus, including the HIV virus, in a cell by administering NDGA or a derivative of NDGA to the cell.
CN1772063A Inner pile treating orally taken medicine The present invention discloses one kind of inner pile treating orally taken medicine. The medicine is prepared with date and sulphur as material in certain weight ratio and through unique preparation process based on the different characteristics of the medicine materials. The medicine has the advantages of fast acting, fast hemostasis, fast healing and no recurrence.
CN103547273A Pre-filled syringe filling syringe having resin barrel with aqueous solution containing hyaluronic acid or salt thereof Provided is a pre-filled syringe that can stably store a highly-pure sodium hyaluronate aqueous solution that fills the inside of a resin barrel. Provided is a pre-filled syringe that fills a syringe having a resin barrel with an aqueous solution containing hyaluronic acid or a salt thereof. Moreover, the aqueous solution containing hyaluronic acid or a salt thereof contains a divalent soluble iron content of no greater than 5 ppb, and contains at least one additive selected from the group consisting of a metal thiosulfate, a metal thiocyanate, a thiourea, a thiosemicarbazide, a thioketone, and a sulfide.
CN102552158A Metacavir enteric coating pellet and preparation method thereof The invention belongs to the field of medicinal preparations and relates to a Metacavir enteric coating pellet. The Metacavir enteric coating pellet contains a medicine-containing micro-pellet consisting of Metacavir as an active component and a pharmaceutical excipient as well as an enteric-coating layer consisting of acrylic resin substances and other pharmaceutical excipients, wherein an isolating layer is arranged between the enteric-coating layer and a main medicinal layer. The Metacavir enteric coating pellet disclosed by the invention contains the medicine-containing micro-pellet, the isolating layer and the enteric-coating layer in the percentage by weight: in the medicine-containing micro-pellet, the content of the Metacavir is 20-50 percent and the content of the pharmaceutical excipient is 30-50 percent; in the isolating layer, the content of a coating agent is 2-7 percent and the content of an anti-sticking agent is 0-2 percent; and in the enteric-coating layer, the content of an enteric-coating material is 10-40 percent, the content of a stabilizing agent is 0-1 percent, the content of a plasticizer is 1-5 percent and the content of an anti-sticking agent is 3-10 percent. The Metacavir enteric coating pellet prepared by the preparation method disclosed by the invention has the advantages of strong acid resistance, stability in release speed and favorable stability.
US20110251174 2,4-diamino-pyrimidines as aurora inhibitors The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
EP0970243B1 Diagnosis and treatment of glaucoma Methods of diagnosing glaucoma, and particularly primary congenital glaucoma, by detecting mutations in a gene associated with glaucoma, such as the CYP1B1 gene, are disclosed. Methods include hybridization analysis, such as Southern or Northern analysis, which use hybridization of a mutant nucleic acid probe to the gene associated with glaucoma; direct mutation analysis by restriction digest; sequencing of the gene associated with glaucoma; hybridization of an allele-specific oligonucleotide with amplified genomic DNA; or identification of the presence of mutant proteins encoded by the gene associated with glaucoma. Kits for use in diagnosis of glaucoma are also described. Methods of treatment of glaucoma, including administration of the protein encoded by the gene associated with glaucoma; administration of genes, gene constructs, or other nucleic acid constructs; or administration of other therapeutic agents, are additionally described.
US20090163460 Diagnostics and therapeutics for early-onset menopause A method of predicting whether a subject is predisposed to developing early-onset menopause is provided. The method involves genotyping a patient at the IL-1 gene loci.
US6869955 Tetrahydropteridines and pyridylpiperazines for treatment of neurological disorders Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.
WO2011002011A1 Combined medicine of sglt1 inhibitor and dpp-iv inhibitor A medicinal agent useful for the treatment of hyperglycemia-related diseases, which comprises a combination of 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H- pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2- dimethylpropionamide, which has an inhibitory activity on SGLT1 (sodium-dependent glucose cotransporter 1), or a pharmacologically acceptable salt thereof and a DPP-IV inhibitor.
CN1874780A Method of inhibiting the expression of a multi-drug resistance genes and inhibiting the production of proteins resulting from the expression of such genes thereby enhancing the effectiveness of chemot The present invention provides, in one aspect, a method of inhibiting the expression of a multi-drug resistance gene in an animal cell which comprises administering to an animal an effective amount of at least one cholesterol absorption inhibitor. In another aspect, it provides a method of inhibiting the production of a protein expressed by a multi-drug resistance gene in an animal cell which comprises administering to an animal an effective amount of at least one cholesterol absorption inhibitor. In another aspect, the present invention provides a method of enhancing the effectiveness of a chemotherapeutic agent in an animal having cancer, which comprises administering to said animal an effective amount of the chemotherapeutic agent and at least one cholesterol absorption inhibitor. Further, there are provided compositions and kits for use in cancer treatment which comprise at least one chemotherapeutic agent and at least one cholesterol absorption inhibitor.
US8383153 Poly(amidoamine) oligomer hydrogel for drug delivery and drug carrier using the same Disclosed is a temperature- and pH-sensitive hydrogel composed of a poly(amidoamine) oligomer only. The hydrogel is prepared in a simple manner and is readily released from the body. Further disclosed are a method for preparing the hydrogel and a drug carrier using the hydrogel.
CN102670639A Novel application of azithromycin The invention relates to an application of azithromycin or solvate thereof in preparing drugs for treating allergic (anaphylactic) rhinitis. The azithromycin is (2R, 3S, 4R, 5R, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-didanosine-3-C-methyl-3-O- methyl-alpha -L-nucelus- hexose pyranose base) oxygen]-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[(3,4,6-trideoxyhexoses-3-(dimethylamino)-beta-D-wood-hexose pyranose base) oxygen]-1-oxa-6-nitrogen heterocyclic pentadecane-15-ketone.
CN1621036A Powder injection of hydrochloric acid ranitidine and its preparation method The present invention relates to one kind of ranitidine hydrochloride powder for injection and its preparation process. The ranitidine hydrochloride powder for injection of the present invention consists of ranitidine hydrochloride and pharmaceutically allowed injection supplementary material. The ranitidine hydrochloride powder for injection of the present invention has convenience in transportation, long storage life, high stability and high quality, and is suitable for large scale production.
WO2012028663A1 Dry powder inhalation drug products exhibiting moisture control properties and methods of administering the same A drug product comprising: a dry powder inhalation device containing one or more pharmaceutical compositions present therein, wherein the one or more pharmaceutical compositions comprise active ingredients (I) 4-{(1R)-2-[(6-{2-[(2,6- dichlorobenzyl)oxy]ethoxy} hexyl)amino]-1-hydroxyethyl}-2- (hydroxymethyl)phenol, or a salt thereof, and (II) (6α,11ß,16α,17α)-6,9-difluoro- 17-{[(fluoromethyl)thio]carbonyl}-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien- 7-yl 2- furancarboxylate or a solvate thereof; a hygroscopic material; and a package which encompasses the dry powder inhalation device and the hygroscopic material defining an enclosed volume therein; wherein each of the active ingredients (I) and (II) are present in the same or different pharmaceutical compositions, and wherein the enclosed volume within the package exhibits a Relative Humidity of from 20% to 40%.
WO2007002214A3 Acyl guanidines as beta-secretase inhibitors There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2. R3, R4 and R5 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by Beta-secretase and, more specifically, inhibit the production of ABeta-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to Beta-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
CN1817880A 2-bit-substituted quinolone compound and use in pharmacey A 2-bit substituted quinonone compound and its use in pharmacy are disclosed. It has antineoplastic activity and can be used for antineoplastic medicine.
CN102584827A Carbapenem compound containing sulfuryl amine heterocyclic methylamino formoxyl pyrrolidine The invention belongs to the technical field of medicine, in particular to a carbapenem compound containing sulfuryl amine heterocyclic methylamino formoxyl pyrrolidine shown as a general formula (I), a pharmaceutically-acceptable salt thereof, an easily-degradable ester thereof, a stereoisomeride thereof, a solvent compound thereof and an intermediate shown as a formula (II), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are defined as the specifications. The invention further relates to preparation methods of these compounds, a medicinal preparation containing the compounds, and applications of these compounds to preparation of a medicament for treating and/or preventing infectious diseases.
CN103417689A Method for preparing colon-cleansing particles used before labor induction at later stage of pregnancy The invention discloses a method for preparing colon-cleansing particles used before labor induction at the later stage of pregnancy and aims to solve the problem of colon cleansing before labor induction at the later stage of pregnancy. The colon-cleansing particles are characterized by being prepared by the following active pharmaceutical ingredients, by weight ratio, horseweed herb, fructus cinnamomi, red clover, Chinese starjasmine stem, big alpine swertia, four-leaf ginseng, fructus psoraleae, tangerine peel, sunflower flowers, turbo cornutus solander, loranthus parasiticus and magnesium sulfate. The method includes (1), extracting volatile oil from fructus psoraleae, fructus cinnamomi and big alpine swertia coarse powder for standby use; (2), smashing turbo cornutus solander, loranthus parasiticus into fine powder for standby use; (3), adding water in horseweed herb, red clover, Chinese starjasmine stem, four-leaf ginseng, sunflower flowers and tangerine peel for decoction twice, filtering, merging filtrate, concentrating the filtrate, adding ethanol for deposition, taking superlate, recycling ethanol and concentrating to obtain thick paste; (4), adding the volatile oil obtained in step 1, the fine powder obtained in step 2 and magnesium sulfate in the thick paste obtained in step 3, uniformly stirring, forming particles, drying and obtaining the colon-cleansing particles. Clinical experiments show that the colon-cleansing particles has good colon-cleansing effect when used before labor induction at the later stage of pregnancy and are worthy of clinical application and popularization.
EP1115877B1 Polynucleotide constructs and uses thereof A polynucleotide is provided which comprises at least two repeats of a hypoxia response element (HRE), wherein the hypoxia-inducible factor consensus binding sites within each of the two repeats are separated by a spacer of at least 20 contiguous nucleotides. A polynucleotide is also provides which comprised at least three repeats of a phosphoglycerate kinase (PGK) hypoxia response element (HRE) operably linked to an SV40 promoter or an MLV promoter. The polynucleotide may be operably linked to a nucleic acid of interest to drive expression of the NOI in a cell under hypoxic conditions.
CN101496803B Application of compound taurine and ansiolin in preparing medicament for treating brain injury disease The invention discloses application of a taurine and diazepam compound recipe in preparing a medicine for treating ischemic cerebral injury diseases. The taurine and diazepam compound recipe can obviously reduce the neuroethological grade, the water content of the brain and the volume of cerebral infarction, and simultaneously can obviously lighten the denaturation and the necrosis of hippocampalneurons and improve the study and memory functions; and the effect of the taurine and diazepam compound recipe is superior to a taurine single group and a diazepam single group, which shows that taurine and diazepam have certain synergism. Moreover, the dosage of a single medicine under the condition of compound treatment can be obviously less than the dosage of the single medicine under the condition of independent treatment so as to contribute to the reduction of the side effects of the medicines and reinforce the safety of medicine usage. The treatment of the taurine and diazepam compound recipe has obvious synergetic neuroprotective effect on acute and chronic injuries caused by ischemic cerebral injury.
US7498146 Containing high-molecular vWF multimers and being free from low-molecular vWF molecules and proteolytic vWF degradation products; chromatographic purification of Factor VIII or a Factor VIII/vWF-complex, admixing a purified high-molecular fraction of vWF molecules; hemophilia A, von Willebrand Disease There are disclosed a stable factor VIII/vWF-complexes, particularly comprising high-molecular vWF multimers, being free from low-molecular vWF molecules and from proteolytic vWF degradation products, as well as methods of producing these complexes.
US20100113519 1,5-Dideoxy-1,5-imino-D-glucitol Compounds 1,5-Dideoxy-1,5-imino-D-glucitol compounds as shown in the specification. Also disclosed is a method of treating a hexosaminidase-associated disease.
CN101787026A Amorphous entecavir p-toluenesulfonate salt and preparation method and medicament application thereof The invention provides amorphous entecavir p-toluenesulfonate salt with high bioavailability, high stability, high yield and high purity. The amorphous entecavir p-toluenesulfonate salt is determined as an amorphous state of entecavir p-toluenesulfonate salt through detections such as X-ray diffraction, infrared absorption spectrum determined by a KBr tablet method, differential scanning calorimetry (DSC) and the like. The invention also relates to a preparation method and medicament application of the amorphous salt.
CN103127060A Application of chloranthus japonicus alcohol D in preparation of antitumor drugs The invention belongs to the chemical field and medical field, and relates to application of chloranthus japonicus alcohol D in preparation of antitumor drugs. Cancer cells comprise hepatoma carcinoma cells, gastric carcinoma cells, pancreatic cancer cells, cervical cancer cells leukemia cells or breast cancer cells. The chloranthus japonicus alcohol D belongs to natural products, is high in bioavailability, and stable in properties, and has clinical value. Small molecule compounds can be used as new antitumor drugs or auxiliary components of the new antitumor drugs to develop, and are obvious in tumor suppression effects, green, and environment-friendly, and provides a new way and method for treating and curing tumours.
CN102940639A Application of indometacin2-aryl morpholine ethyl ester in preparing medicine capable of resisting breast cancer The invention relates to an application of indometacin2-aryl morpholine ethyl ester or salt thereof disclosed in a chemical structural formula I in preparing a medicine capable of resisting the breast cancer. In the chemical structural formula I, R is selected from nitrogen and C1-C4 alkyl, Ar is selected from phenyl, substituted phenyl, naphthalene-1-base, naphthalene-2-base or substituted naphthyl, and salt is selected from hydrochloride, hydrobromide, sulfate, phosphate, mesylate, benzene sulfonate, tosilate, malate, maleate, citrate, tartrate or lactate.
CN103432161A Multivitamin mineral effervescent tablet and preparation method thereof The invention discloses a multivitamin mineral effervescent tablet which comprises the following components in parts by mass: 60-80 parts of ferrous gluconate, 50-70 parts of zinc gluconate, 0.03-0.08 part of sodium selenite, 0.08-1.6 parts of vitamin B1, 0.08-1.6 parts of vitamin B2, 0.08-1.5 parts of vitamin B6, 70-90 parts of vitamin C, nicotinic acid, pantothenic acid, folic acid, organic acid, carbon dioxide source, acid particle binder, lubricant, alkali particle filler, corrigent, microcrystalline cellulose, fruit powder and sorbitol. The multivitamin mineral effervescent tablet contains multiple mineral matters and multiple vitamins and is a multivitamin mineral effervescent tablet with the combination of multiple vitamins and mineral matters. The invention further discloses a preparation method of the multivitamin mineral effervescent tablet.
US20080032976 Histamine 3 receptor antagonists and/or inverse agonists; for obesity, metabolic syndrome (syndrome X), and other eating disorders; (4-cyclopentyl-piperazin-1-yl)-[3-(1-isopropyl-piperidin -4-yl)-l H-indol-6-yl]-methanone The present invention relates to the compounds of formula I: wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
US20120322783 Tumescent antibiotic solution Disclosed herein are solutions and kits for tumescent antibiotic delivery. Embodiments of the solution comprise an antibiotic component, an anesthetic component and a vasoconstrictor component. In addition, a method of use is disclosed comprising subcutaneous delivery of the solution. The disclosed solution, kit and method of subcutaneous delivery can be used for a variety of surgical procedures including liposuction, mastectomy and others. The tumescent antibiotic solution can be administered to a patient in situations where establishing IV access is difficult, impossible, or undesirable. A variety of delivery methods appropriate for surgical settings, as well as for use by first responders are likewise disclosed.
US20090035224 Methods of Using Albuterol and Calcium Activated Potassium Channel Openers This invention related to methods of treating, preventing and managing various pulmonary or respiratory diseases or disorders using albuterol in combination with calcium activated potassium channel openers. Pharmaceuticals compositions comprising albuterol and calcium activated potassium channel openers are also disclosed.
WO2007122634A2 Pyrimidinediones as tyrosine kinase inhibitors The present invention relates to a compound of formula (I) or its stereoisomers, tautomers, solvates, hydrates, prodrugs, pharmaceutically acceptable salts or mixtures thereof, wherein A1 is nitrogen; A2 is carbon; Rl is independently selected from the group consisting of aryl or 5-6 membered heterocyclic ring system; R2 and R3 are independently selected from the group consisting of H, alkyl, substituted alkyl, alkylaryl, alkylheteroaryl, aryl, or 5-6 membered heterocyclic ring system; provided R2 or R3 is H. The present invention also provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier or diluents. The present invention also provides a method for the prophylaxis or treatment of a medical condition associated with protein kinase, by administering a pharmaceutically effective amount of the compound of formula (I) or salts thereof.
WO2013040556A1 Compositions of jasmonate compounds and methods of use The disclosure describes nanocarried and/or microcarried jasmonate compounds and their pharmaceutical compositions, as well as use thereof for treating or preventing angiogenesis- related or NF-κB-related disorders. Also disclosed are methods of making the nanocarried and/or microcarried compounds and their compositions.
WO2014116132A1 Biomaterial comprising poly(trimethylene carbonate-co-e-caprolactone) for promoting axonall growth and neuronal regeneration Mammalian central nervous system (CNS) neurons do not regenerate after injury due to the inhibitory environment formed by the glial scar, largely constituted by myelin debris. The use of biomaterials to bridge the lesion area and the creation of an environment favoring axonal regeneration is an appealing approach, currently under investigation. This work aimed at assessing the suitability of three candidate polymers - poly(?-caprolactone), poly(trimethylene carbonate-co- ?-caprolactone) (P(TMC-CL)) (11:89 mol%) and poly(trimethylene carbonate) - with the final goal of using these materials in medicine, namely in the development of conduits to promote spinal cord regeneration. Cortical neurons cultured on P(TMC-CL) in the presence of myelin were able to tame myelin inhibition in comparison with the control condition (glass substrate). This effect was found to be mediated by the glycogen synthase kinase 3p (GSK3p) signaling pathway with impact on the collapsin response mediator protein 4 (CRMP4), suggesting that nanomechanical properties were implicated in this process. The obtained results indicate P(TMC-CL) as a promising material for CNS regenerative applications as it promotes axonal growth, taming myelin inhibition.
WO2010043186A1 New pt(ii) complex and antitumor activity thereof The present invention provides a Pt(II) complex comprising 3-aza-1,1-cyclosuccinic acid or its derivative as ligand, and provides the antitumor activity of the typical compounds.
EP2682119A1 Aromatic N-heterocycle derivatives for use as medicine The invention relates to compounds, or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal thereof, wherein said compound is of formula A-B (I) wherein A is substitued or not aromatic N-heterocycle; and B is -[C(R1)(R2)]n-R3 wherein n is an integer between 1 and 10, R1 and R2 represent independently in each of the n units a substituent selected from the group consisting of hydrogen, substituted or not C1-C10 alkyl, halogen, oxy derivatives, thioderivatives, substituted or not C3-C10 cycloalkyl, substituted or not C6-C18 aryl, substituted or not C2-C10 alkenyl, substituted or not C2-C10 alkynyl, R3 represents a substituent selected from the group consisting of hydrogen, substituted or not C1-C10 alkyl, halogen, substituted or not C3-C10 cycloalkyl, substituted or not C6-C18 aryl, substituted or not C2-C10 alkenyl, substituted or not C2-C10 alkynyl, amino, heterocycle, thiocyanate, thio derivatives, hydroxylamine, amido, sulfonamide, amino sulfone derivatives, ether, thioether, ester, thioester, azido, azo, cyano, nitro, nitrooxy, carbamate, thiocarbamate, sulfinyl derivative, sulfonyl derivatives, acyl derivatives, oxy derivatives, ureido, thioureido, imino, oximino, hydrazino, thioamido, carboxylic, phosphate, phosphonate, carbamoyl phosphate; with the proviso that when A is 5-fluoroindole, B is bonded at position 3 of the 5-fluoroindole moiety, R1 is hydrogen and n is between 2 and 10, R3 is not -NR4R5 wherein R4 and R5 independently represent a substituent selected from the group consisting of hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl, aminoalkyl, or R4 and R5 taken together with the nitrogen atom to which they are attached to form a four to ten-membered heterocycle, and R2 is not independently in each of the n units a substituent selected from the group consisting of hydrogen, C1-C10 alkyl, halogen, alkoxy, aminoalkyl, and alkylamino; for the treatment or the prophylaxis of neurologic and/or inflammatory diseases or disorders. The present invention also provides pharmaceutical composition and in vitro method for inhibiting myeloperoxidase enzyme activity or low density lipoproteins oxidation.
CA2713679A1 Orally rapidly disintegrating tablet comprising imidafenacin Provided herein is an imidafenacin-containing orally rapidly disintegrating tablet which is excellent in the photostability. The orally rapidly disintegrating tablets comprises (1) a granulated product containing imidafenacin or imidafenacin particles, which is or are coated with povidone or a gastric juice-soluble polymer; and (2) a composition containing an excipient and a disintegrating agent, wherein the resulting composition is subjected to compression molding.
CN101836996A Oral solid preparation using loperamide hydrochloride and simethicone as main ingredients The invention relates to an oral solid preparation using loperamide hydrochloride and simethicone as main ingredients. In the preparation, the loperamide hydrochloride and simethicone and pharmaceutically acceptable auxiliary materials of the loperamide hydrochloride and simethicone are used to prepare the solid preparation by pharmaceutical technology. The oral solid preparation of the invention is stable and controllable in quality, safe and effective.
US7345090 Galenical formulation The invention relates to compounds of the formula I where R1, R2, R3, R4 and R5 have the meanings given in claim 1. The compound is suitable in particular for use in skin care compositions. They protect, firstly, against harmful oxidation reactions and, secondly, also act as UV filters.
US20080274177 Monolithic coating comprising aqueous dispersion of neutral acrylic ester copolymer without any functional groups and polyglycol; short curing times; shelf life The invention provides stable controlled release monolithic coating compositions for use in coating pharmaceutical oral dosage forms comprising a polyglycol having a melting point greater than 55° C. and an aqueous dispersion of a neutral ester copolymer lacking functional groups.
EP2374461A1 Piroxicam for prophylactic and therapeutic treatment of herpes infections Agent comprises piroxicam in a carrier substance. - ACTIVITY : Virucide; Antirheumatic. - MECHANISM OF ACTION : Cyclooxygenase inhibitor.
US20100113613 cyclohexane polyalcohol formulation for treatment of disorders of protein aggregation The invention provides formulations, dosage forms, and treatments comprising cyclohexane polyalcohol compounds that provide beneficial pharmacokinetic profiles in the treatment of a disorder and/or disease including a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence. In aspects of the invention, a dosage form is provided comprising an amount of a cyclohexane polyalcohol compound suitable for administration to a subject to provide a therapeutically effective concentration of the compound in plasma, brain and/or cerebral spinal fluid and a pharmaceutically acceptable carrier, diluent or excipient. The formulation can be administered in a dose of 500, 1000, 2000, 3500, 5000 or 7000 mg of cyclohexane polyalcohol compound to achieve a mean plasma concentration profile having a mean AUC0-INF in μ·h/mL of, respectively, 43±20%, 130±20%, 215±20%, 467±20%, 507±20% or 885±20%, and having a mean Cmax in μmL of, respectively, 5.8±20%, 17±20%, 33±20%, 75±20%, 110±20% or 155±20%.
US20070207229 Inhibitor of blood glucose level elevation and inhibitor of age generation comprising acerola leaf extract and food product comprising either thereof This invention is directed to providing an inhibitor of blood glucose level elevation and an inhibitor of AGE generation made from natural ingredients and a food product comprising either thereof. Such inhibitor of blood glucose level elevation or inhibitor of AGE generation comprises, as an active ingredient, an acerola leaf extract and/or a processed product thereof.
WO2012094966A1 3-aryl-6-aryl-[1,2,4]triazolo[4,3-b]pyridazine as cell proliferation inhibiting agent and use thereof Provided is a novel 3-aryl-6-aryl-[1,2,4]triazolo[4,3-b]pyridazine represented by Formula I, wherein Ar1, Ar2, and R1-R2 are as defined herein. The compound of Formula I is a cell proliferation inhibiting agent. Therefore, the compound of the present invention is useful for treatment of diseases caused by uncontrolled abnormal cell growth and spreading.
CN1943563A Vitamin dripping pill and its preparing method The invention related to vitamin drop pills and its preparation process and belongs to technical field of drug preparation. Its formula consists of vitamin, base material for drop pills, anti-oxidant, surface active agent, coating material, etc. its process is first prepared vitamin into farine with fineness above 150 mesh. Take base material of formula and soluble after heating, adding vitamin farine and relevant auxiliary material, mixing into even dispersible solution, dropping into condenser and becoming pills, preparing into pills with coating or non-coating. Each pill containing vitamin 0.05mg-30mg and its weight is 10mg-100mg.
EP1098885B9 Imidazole compounds and their use as adenosine deaminase inhibitors Imidazole compounds having adenosine deaminase inhibitory activity represented by formula (I) wherein R1 is hydrogen, hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent (s); R2 is hydrogen or lower alkyl; R3 is hydroxy or protected hydroxy; R4 is cyano, (hydroxy)iminoamino(lower)alkyl, carboxy, protected carboxy, heterocyclic group optionally substituted with amino, or carbamoyl optionally substituted with suitable substituent(s); and -A- is -Q- or -O-Q-, wherein Q is single bond or lower alkylene, provided that when R2 is lower alkyl, then R1 is hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s), its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.
EP1682115A2 Hif-1 inhibitors and methods of use thereof Methods of treating cancers or tumor, chemopreventative methods of prophylactically treating cancers or tumors, pharmaceutical compositions, methods for the treatment or prevention of a hypoxia-related pathology, methods of modulating HIF-1 activity in a cell, methods of downregulating HIF-1 activity I a cell, methods of treating or preventing cancer or a tumor in a host, and methods of modulating gene transcription in a cell are described.
CN1857272A Alprostadil infusion solution and its preparing method The present invention discloses a kind of alprostadil infusion solution and its preparation process. The alprostadil infusion solution consists of alprostadil, emulsifier, triglyceride, osmotic regulator, stabilizer, antioxidant, and pH regulator in certain proportion. The preparation process includes mixing alprostadil, emulsifier, triglyceride and stabilizer and dissolving to form oil phase; dissolving water soluble components, glycerine, etc in water to obtain water phase; adding the water phase into the oil phase, emulsifying in an ultrasonic apparatus or homogenizer and regulating pH to 4-9 to obtain initial emulsion; further emulsifying to obtain emulsion; sterilizing and filtering with 0.22 nm, packing and sterilizing to obtain the alprostadil infusion solution.
WO2013091657A1 Therapeutic applications of calcium electroporation to effectively induce tumor necrosis The present inventors have shown that electroporation with calcium ions are efficient on cutaneous and subcutaneous nodules. In particular the present inventors here disclose that a solution comprising calcium ions (Ca2+) with a concentration of at least 0.1 M is extremely useful in a method of treating a neoplasm, such as cancer with means for causing transient permeabilisation of the cell membranes of at least part of the neoplasm before, during and/or after administration of said solution,wherein said solution is administered with a ratio of 0.2 to 0.8 of the volume of said part of the neoplasm.
EP2711004A1 Methods for increasing physical capacity of mammalian livestock The present invention relates to a method for increasing physical capacity of mammalian livestock comprising administering to the mammalian livestock a composition comprising choline, palmitate, vitamin C and vitamin E.
CN101274100A Method for preparing adriamycin-dipeptide complexes and applications The invention discloses a preparation method of an adriamycin-dipeptide compound. Dipeptide or polypeptide containing proline residue is connected to amino of the adriamycin by the acylation through the technique of peptide modification; the toxicity of the adriamycin can be reduced and at the same time the pro-drug can release the adriamycin under the action of tumor interstitial cells so as to ensure that the adriamycin can enrich around tumor tissue to improve the selectivity of the adriamycin to the tumor tissue. The preparation method of the invention has the advantages of fast reaction rate, short term, relatively high productive rate and purity.
WO2005123193A3 Treatments comprising strontium for rheumatic and arthritic diseases and pain Improved treatments of joint diseases, such as, e.g. osteoarthritis and rheumatoid arthritis, and pain, wherein a strontium-containing compound is administered alone or in combination with one or more second therapeutically and/or prophylactically active substances, selected from the group consisting of bisphosphonates, glucosamine, pallitative agents, analgesic agents, disease modifying anti-rheumatic compounds (DMARDs), selective estrogen receptor modulators (SERMs), aromatase inhibitors, non-steroidal anti-inflammatory agents (NSAIDs), COX-2 inhibitors, COX-3 inhibitors, opioids, inhibitors/antagonists of IL-1, inhibitors/antagonists of TNF-α, inhibitors of matrix metallo-proteinases (MMPs), cathepsin K inhibitors, inhibitors/antagonists of RANK-ligand, statins, glucocorticoids, chondroitin sulphate, NMDA receptor antagonists, inhibitors of interleukin-I converting enzyme, Calcitonin gene related peptide antagonists, glycine antagonists, vanilloid receptor antagonists, inhibitors of inducible nitric oxide synthetase (iNOS), N-acetylcholine receptor agonists, neurokinin antagonists, neuroleptic agents, PAR2 receptor antagonists and anabolic growth factors acting on joint tissue components. Pharmaceutical compositions comprising a strontium-containing compound and a second therapeutically and/or prophylactically active substance as defined above.
CA2182228C Codrugs as a method of controlled drug delivery A codrug composition of at least two drug compounds covalently linked to one another via a labile bond to form a single codrug composition and methods of use of the codrug for the treatment of various medical conditions. The codrug may be administered by itself or in the form of a bioerodible or nonbioerodible substance.
EP1844027A1 Thiazolidinones for use as inhibitors of polo-like kinase (plk) The invention relates to the thiazolidinones of general formula (I), to the production and use thereof as inhibitors of Polo-like kinase (Plk) for use in the treatment of various diseases.
CN101011356A Aerosol and its preparation The invention relates to a method for preparing aerosol, which comprises 0.20-0.50mg/ml opitum receptor antagonist or relative acceptable salt, 0.025-0.050mg/mL oleic acid, 0.30-0.60mg/mL trichloromonofluoromethane, and 1.00-1.50mg/mL dichlorodifluoromethane. The invention also provides relative preparation, while the aerosol can be used in wine relieving and drug rehabilitation.
CN101906128A Estrone compound, as well as preparation method and application thereof The invention relates to a novel estrone compound, a preparation method of the compound, and application of the compound as a selective extrogen receptor regulator to the preparation of medicaments for treating and/or preventing osteoporosis, improving woman menopausal syndrome, and relevant diseases.
CN103656361A Medicine used for treating herpes zoster, and preparation method thereof The invention discloses a medicine used for treating herpes zoster, and a preparation method thereof. The medicine is prepared from medical ingredients, such as herba portulacae, semen plantaginis, oldenlandia diffusa, radix gentianae, rheum officinale, herba violae, rulvis glycyrrhizae extractionis sedilis, radix salviae miltiorrhizae, yam rhizome and complete scorpion, according to a certain weight ratio. The medicine is capable of clearing away heat and toxic materials, dispersing blood and diminishing swelling, and diminishing inflammation and killing parasite; and can be used for treating herpes zoster with rapidly realized effects and excellent curative effects; and relapse of herpes zoster is seldom caused.
WO2008044785A1 Material for improvement of cerebral blood flow, and use thereof Disclosed is a material for improving the cerebral blood flow, which comprises a plant-derived carbon fiber. The material produces no adverse side-effect and is therefore safe, and can improve the cerebral blood flow effectively. Also disclosed is use of the material.
US20120165349 Phenyl-Substituted Pyrazolopyrimidines The invention relates to novel phenyl-substituted pyrazolopyrimidines, process for their preparation, and their use for producing medicaments for improving perception, concentration, learning and/or memory.
US8722866 Isoform-selective inhibitors and activators of PDE3 cyclic nucleotide phosphodiesterases The present invention concerns methods and compositions related to type 3 phosphodiesterases (PDE3). Certain embodiments concern isolated peptides corresponding to various PDE3A isoforms and/or site-specific mutants of PDE3A isoforms, along with expression vectors encoding such isoforms or mutants. In specific embodiments, methods for identifying isoform-selective inhibitors or activators of PDE3 are provided, along with methods of use of such inhibitors or activators in the treatment of dilated cardiomyopathy, pulmonary hypertension and/or other medical conditions related to PDE3 effects on cAMP levels in different intracellular compartments.
US7179818 Substituted aminoquinuclidine compounds This invention is directed towards substituted aminoquinuclidine compounds useful as delta-opioid receptor modulators, delta-opioid receptor agonists useful as analgesics and delta-opioid receptor antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
US20090092656 Method of treating atrophic vaginitis The present invention provides novel pharmaceutical compositions containing triphenylethylene derivative compounds, and methods of using the composition for treatment of symptoms associated with atrophic vaginitis. The pharmaceutical compositions are prepared for the vaginal administration of triphenylethylene derivative compounds in single or combination therapies. Preferably, the triphenylethylene derivative is tamoxifen.
CN101845044A New crystal forms of Abafungin and preparation method thereof The invention belongs to the technical field of pharmaceutical chemistry, in particular to two new crystal forms of Abafungin N-[4-[2-(2,4-dimethylphenoxy)phenyl]-2-thiazolyl]-1,4,5,6-tetrahydro-2-Pyrimidinamine as an antifungal medicament and, a preparation method thereof as well as, a medicament composition containing the two new crystal forms and the application of the two new crystal forms in manufacturing the antifungal medicament.
EP2560660A1 Chemosensory receptor ligand-based therapies Provided herein are compositions and methods for treating diabetes, obesity, and other metabolic diseases, disorders or conditions with chemosensory receptor ligands. Also provided herein are pharmaceutical compositions useful for the methods of the present invention.
US20050271669 For therapy of proliferative disease The invention relates to a pharmaceutical combination which comprises (a) a HER-1 or a HER-2 antibody or (b) at least one antineoplastic agent selected from the group consisting of aromatase inhibitors, antiestrogens, topoisomerase I inhibitors, topoisomerase II inhibitors, microtubule active agents, protein kinase C inhibitors, anti-angiogenic compounds, gonadorelin agonists, anti-androgens, histone deacetylase inhibitors and S-adenosylmethionine decarboxylase inhibitors; and (c) an epothilone derivative of formula I and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular, for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
US20100330194 Silicon Substituted Phosphates The invention is various applications of silicon substituted phosphates of various chemical composition and granular sizes in direct application or in combination with other materials, not previously claimed in prior art used to treat the various medical conditions described.
US20110212941 Imidazoisoindole Neuropeptide S Receptor Antagonists The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
US20100267660 microorganism comprising a heterologous gene encoding a bifunctional Campylobacter jejuni sialytransferase polypeptide and which lacks Neu5Ac aldolase activity and beta galactosidase activity; treating Miller Fisher syndrome The present invention relates to the enzymatic synthesis of oligosaccharides, particularly, sialylated oligosaccharides comprising the carbohydrate moeities of the gangliosides GM3, GD3, and GT3.
CA2780333A1 1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties The present invention provides novel chemical compounds characterized as Rho kinase (ROCK) inhibitors, methods for their discovery, and their therapeutic, research, and diagnostic use. In particular, the present invention provides 1,4-benzodiazepine-2,5-dione compounds and related compounds having ROCK inhibitory activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with ROCK activity.
US20080274991 Nucleic Acids Against Viruses, in Particular Hiv The invention provides a nucleic acid molecule comprising a sequence that is complementary to a mutant of a genomic nucleic acid sequence of an organism capable of mutating its genome. The genomic nucleic acid sequence preferably comprises a conserved, essential region. Furthermore, the genomic nucleic acid sequence preferably comprises a coding sequence and a DNA/RNA regulatory sequence. A pharmaceutical composition and a gene delivery vehicle comprising a nucleic acid molecule of the invention is also provided, as well as a method for counteracting an organism comprising providing the organism with the nucleic acid molecule. The organism is preferably additionally provided with a nucleic acid sequence complementary to a genomic nucleic acid sequence of the organism.
US20050261260 Combination of a CDK inhibitor and mitoxantrone A first aspect of the invention relates to a combination comprising a CDK inhibitor and mitoxantrone. A second aspect of the invention relates to a pharmaceutical product comprising a CDK inhibitor and mitoxantrone as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a CDK inhibitor and mitoxantrone to a subject.
US20100029598 Extended Benzamide Derivatives as Modulators of the EP2 Receptor The present invention relates to extended benzamide derivatives of the general formula I, to processes for preparation thereof and to use thereof for production of pharmaceutical compositions for treatment of disorders and indications associated with the EP2 receptor.
CN1830435B Oleanol type benzofuran and its glucoside applied in preparation of anti female hormone deficiency medicine An application of oleanolic benzifuran and its heteroside in preparing the medicine for treating estrin deficiency, ovarian function sanilism, polycystic ovarian syndrome, climacteric syndrome, osteoporosis, ovarian hypofunction, etc, and the medicine in the form of tablet, capsule, etc are disclosed.
US20080279817 Treatment of Autoimmune Diseases and Allograft Rejection with IL-21 The invention provides combination treatments with IL-21, an analogue, a derivative or active fragment thereof, an IL-21 mimetic or IL-21 polynucleotide.
EP2611437A1 Pharmaceutical composition for prevention and treatment of amyotrophic lateral sclerosis The present invention provides a prophylactic or therapeutic agent for amyotrophic lateral sclerosis, containing a 1,3-diphenylurea derivative or multikinase inhibitor.
CN102973689A High effect suppurative otitis powder and preparation method thereof The present invention relates to special high effect suppurative otitis powder for suppurative otitis media treatment and a preparation method thereof. The high effect suppurative otitis powder is characterized in that the powder comprises the following raw materials, by weight, 15-20 parts of fried rheum powder, 15-20 parts of fried longleaf garden burnet root powder, 16-22 parts of borax, 16-22 parts of weathered sodium sulfate, and 11-16 parts of borneol. The preparation method comprises: frying rheum and longleaf garden burnet root into a brown color, wherein a certain drug nature is remained; respectively grinding and screening through a 180 mesh sieve, and weighing the rheum powder and the longleaf garden burnet root powder according to a certain weight ratio to be spare; weighing borax, weathered sodium sulfate and borneol according to a certain weight ratio to be spare; finally uniformly stirring the weighed rheum powder, the weighed longleaf garden burnet root powder, the borax powder, the weathered sodium sulfate and the borneol powder, filling into a bottle, sealing to obtain the finished product, and placing in a cool place to be spare. The high effect suppurative otitis powder has good effects of heat clearing, blood cooling, bacterial resistance, detoxifying, convergence and tissue regeneration promoting, wherein suppurative otitis media can be cured after use of the high effect suppurative otitis powder 1-2 times.
US20100247652 Alginate Biomaterials for the Treatment of Hepatic Disorders The present invention relates to methods for the treatment of hepatic disorders in a subject in need thereof. More specifically, the methods of the invention are based on the administration, preferably, systemic administration, of a therapeutically effective amount of at least one biocompatible alginate biomaterial, any modification thereof and any combination thereof. The invention further provides methods for sustaining serum albumin levels, and/or reducing serum AST and ALT, in subjects suffering from hepatic disorder. Still further, the invention provides methods for reducing apoptosis and inducing cell proliferation in a damaged liver tissue of a subject suffering of hepatic disorder, using the alginate biomaterial described by the invention.
WO2010041288A1 Use of l-kynurenine and derivatives thereof for the prevention and treatment of diabetes mellitus type 1 Use of L-kynurenine and derivatives thereof for the prevention and treatment of diabetes mellitus type 1 The present invention concerns the use of L- kynurenine or natural or synthetic derivatives thereof, alone or in combination with a ligand of Toll -like receptor for the prevention and treatment of type 1 diabetes mellitus.
US20120237601 Pharmaceutical Compositions Comprising Mycophenolic Acid or Mycophenolate Salt The invention provides a solid dosage form, e.g. a tablet, comprising mycophenolic acid or mycophenolate salt and a process for its production.
EP1337850B1 Method for diagnosing a tumor in a patient determining the concentration of pibf The present invention relates to a method for diagnosing a tumor in a patient said method comprising measuring the concentration of Progesterone-Induced Immunomodulatory Protein (PIBF) or a derivative thereof or a fragment thereof in the sample taken from the patient, and to the use of an anti-PIBF antibody, PIBF or a derivative thereof or a fragment thereof, and a polynucleotide encoding PIBF, respectively, as an anti-tumor medicine.
WO2012008788A3 Composition containing serine as an active ingredient for the prevention and treatment of fatty liver diseases, and use thereof The present invention relates to a composition for the prevention and treatment of fatty liver diseases, containing serine as an active ingredient. The transcription of a transcriptional regulatory factor for fatty acid biosynthesis, which is activated by alcohol according to the present invention, is inhibited in order to inhibit the accumulation of neutral fat in liver tissue, and thus can be effectively used as a composition for the prevention or treatment of fatty liver diseases, or as a functional health food.
US20120083466 Lipid conjugates in the treatment of allergic rhinitis Provided herein are methods of treating, suppressing, inhibiting, or preventing allergic rhinitis in a subject comprising the step of administering to a subject a compound comprising a lipid or phospholipid moiety bond to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.
CN103446106A Applications of Sarcaboside B in antibacterial medicament The invention relates to applications of Sarcaboside B in preparing an antibacterial medicament, and belongs to the field of medicines. The Sarcaboside B plays a strong role in inhibiting escherichia coli, pseudomonas fluorescens, staphylococcus aureus, proteus and cryptococcus neoformans, thus being capable of serving as an antibacterial compound, and being expected to be applied in preparing related medicaments. The applications of the Sarcaboside B in preparing the antibacterial medicament are disclosed for the first time. As a skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpectedly strong bacteria inhibition activity, and the possibility of giving any inspiration by other compounds does not exist. The Sarcaboside B has significantly substantive characteristics, as well as obviously prominent progress in the prevention and treatment of the bacteria infection.
CN1682719B Enteric soluble coating slow releasing tablet containing huperzine A and preparing method The present invention discloses a kind of slow releasing enteric soluble coated tablet containing hyperzine A and its preparation process. Enteric soluble coating technology is adopted to overcome thebad effect of lower pH in stomach on the diffusion of medicine in skeleton tablet to ensure the stable, slow and complete release of medicine. The slow releasing tablet contains hyperzine A as reversible anticholinesterase and has one layer of enteric soluble polymer film coating outside the skeleton slow releasing layer. The active medicine component may be also various pharmaceutically acceptable acid salts of hyperzine A. Each tablet contains hyperzine A I n10-500 microgram and has sustained release time of 20 hr.
CN101259114A Vaginal effervescence tablet composition containing solid lipid The invention provides a vaginal effervescent tablet composition that comprises 100 weight portions of active drug ingredients and 20-1000 weight portions of solid lipid. The vaginal effervescent tablet composition of the invention can be released in vagina slowly and continuously, ensuring that the sufferer feels comfortable, and generates foams that can ensure fine drug powder to be uniformly distributed, leading the drug to be uniformly distributed in the inner wall mucosa of the vagina; meanwhile, the foams last for a long time, which prolongs dramatically the even contact time of the drug and the mucosa of the vagina and extends the effect of the drug; furthermore, the vaginal effervescent tablet composition is easily washed out and more beneficial to the health of sufferers.
CN102153577A 2-seleno-N-pyridine oxide-rare earth metal ion compound and preparation method and application thereof The invention discloses a 2-seleno-N-pyridine oxide-rare earth metal ion compound and a preparation method and application thereof. In a formula shown in the specifications, M is a Yb<3+>, Pr<3+> and Gd<3+> ion. The preparation method has the advantages of cheap raw materials, mild condition, easiness and convenience for operation, high yield and environmental friendliness. The compound can be applied to bacteriostasis, sterilization and anticancer medicaments.
DE20321227U1 New isostructural pseudopolymorph of 9-deoxo-9a-aza-9a-methyl-9a-homo erythromycin A useful for treating e.g. bacterial and protozoal infections An isostructural pseudopolymorph of 9-deoxo-9a-aza-9a-methyl-9a-homoe rythromycin A is new and has the monoclinic space group, average unit cell parameters as given in the specification. An isostructural pseudopolymorph of 9-deoxo-9a-aza-9a-methyl-9a-homoe rythromycin A of formula (I) is new and has the monoclinic space group, average unit cell parameters as given in the specification. [Image] S1an organic solvent which is at least partially miscible with water; x : 1, 1.25, 1.5 or 2; y : 0, 0.5 or 1. An independent claim is also included for preparation of (I). - ACTIVITY : Antibacterial; Protozoacide; Antiinflammatory. No biological data given. - MECHANISM OF ACTION : None given.
US20140080876 Antimicrobial and radioprotective compounds The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above. Some of the compounds of formula (I) are novel and are also described in the present invention, together with pharmaceutical or veterinary compositions containing them.
EP2669271A1 Indole derivative, and pharmacologically acceptable salt thereof The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: [wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents -C(=O)-NH-SO2-R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
EP1253917B1 Use of substituted 4-amino-1-phenylbutan-2-ol compounds as medicaments The invention relates to the use of substituted 4-amino-1-phenylbutan-2-ol compounds in the form of their racemates, enantiomers, diastereomers or corresponding bases or corresponding salts of physiologically acceptable acids as regulators for the nociceptin/orphanin-FQ ligand ORL1 receptor system and for the production of medicaments.
US20110184071 process for the preparation of amines The present invention relates to an improved process for the preparation of rasagiline (1) and its pharmaceutically acceptable salts. In particular it relates to a process for preparing rasagiline (1) and its salts substantially free from impurities.
US20070232796 Medical Solution, a Method for Producing Said Medical Solution and Use Thereof The present invention relates to a medical solution comprising a first single solution containing glucose and/or glucose-like compound. According to the present invention said first single solution has a pH in the range of 1.8-2.6. The present invention further relates to a method for producing said medical solution as well as use thereof.
EP1472249B1 Xanthene-carboxylic acid esters of tropenol and scopine as m3 antagonists, method for producing the same and use thereof as medicaments The invention relates to novel xanthene-carboxylic acid esters of general formula (1), in which X and the groups A, R, R1, R2, R3, R3', R4 and R4' are defined as per the claims and the description. The invention also relates to a method for producing said esters and to the use thereof as medicaments.
CN102335162A Application of trichostatin A (TSA) to preparation of medicament for inhibiting activities of swine ovary granular cells The invention belongs to the field of medicaments and veterinary medicines and discloses application of trichostatin A (TSA) to preparation of a medicament for inhibiting activity of swine ovary granular cells. In the invention, the influence of the TSA to the activities of the swine ovary granular cells is systemically studied, and a result shows that the TSA has no influence to the growth of the swine ovary granular cells at low concentration (below 10ng/mL), with the increase of the concentration, the growth of the swine ovary granular cells is inhibited (P<0.05), and the inhibition effect is dose-dependent. After the granular cells are treated by using 200ng/mL TSA, the cell cycle is retardant within a period G0/G1, and the marked decrease of gene expression of Cyclin D2 and CDK4 (Cyclin-Dependent Kinase 4) is possible to be an important reason for the cycle retardance. Accordingly, the TSA can be applied to preparation of the medicament for inhibiting the activities of the swine ovary granular cells.
US20090053273 Topical medication garment and system and method for providing topical medication A topical medication garment, a system and a method provide topical medication. An impermeable garment may allow the topical medication to maintain contact with the skin of the user. The garment may prevent the topical medication from absorption into clothing or the undergarment itself. The entirety of the garment may be made from an impermeable material or a portion of the garment may be made from an impermeable material. An impermeable liner may be attached to and/or may be connected to an interior surface of the garment. The garment may have legging portions that reside on the upper thighs of the user when the garment is worn. The legging portions may secure the position of the garment on the user and providing coverage of topical medication applied to the crotch area and upper thighs. The garment may have a structure that resembles a t-shirt.
WO2006104137A1 Sucrase activity inhibitor, glucoamylase activity inhibitor and food and feed containing the same The invention provides a sucrase activity inhibitor and a glucoamylase activity inhibitor comprising one or more saccharides selected from the group consisting of palatinose, trehalose and reduced palatinose. Further, the invention provides a food and a feed containing the sucrase activity inhibitor and/or the glucoamylase activity inhibitor.
EP0984930B1 2-indolinone derivatives as modulators of protein kinase activity The present invention relates to novel 2-indolinones and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
WO2010007756A1 Pyridine derivative having ttk inhibition activity The object aims to provide an effective inhibitor of TTK protein kinase and an effective anti-cancer agent. The object can be achieved by a compound of the invention and inventions related to the compound (e.g., a pharmaceutical composition, a TTK inhibitor). A novel series of compounds having specific properties which are particularly useful for the preparation of a medicinal product for inhibiting the activity of TTK kinase to treat the diseases can be successfully found. Particularly, the compound is useful for the treatment of proliferative diseases (e.g., cancer) which occur in the form of a solid tumor or a hematologic tumor and in which it is known that TTK kinase is active. The compound is particularly useful for diseases including colorectal cancer, breast cancer, lung cancer, prostate cancer, pancreatic cancer, bladder cancer, renal cancer, leukemia, lymphoma and others.
US20090042823 Uses of broad spectrum rnai therapeutics against influenza Methods and uses of RNAi-inducing agents for medicaments and treating or preventing a viral infection.
US20100239566 Enigma-mdm2 interaction and uses thereof The present invention relates to Enigma (PDLIM7)-Mdm2 interaction and use thereof. More particularly, it may induce an effective apoptosis of cancer cells by inhibition of an Enigma expression or an Enigma activity which induces Mdm2 destabilization and p53 activity; it may assess the prognosis of anti-cancer therapy by determining that Enigma, which is induced by SRF, is overexpressed in cancer tissues with Mdm2; it may screen anti-cancer activity substances by to selecting a factor to inhibit specific binding between Enigma and Mdm2. Enigma-Mdm2 interaction and Enigma expression regulation may be utilized usefully for preventing cancers and developing therapeutic methods and anti-cancer agents.
EP1968963B1 Substituted propiolic acid amides and their use for producing analgesics The invention relates to the substituted propiolic acid amides of general formula (I), to methods for producing them, to drugs containing said compounds and to the use thereof for producing drugs.
CN101601726A Medicinal composition for reducing blood sugar The invention discloses a medicinal composition for reducing blood sugar, which comprises mulberry leaf, vitamin A, beta-carotene, vitamin B complex, vitamin C, vitamin D, vitamin E, macroelements, namely calcium, potassium and magnesium, and microelements, namely zinc, selenium, iron, chromium, copper, molybdenum, iodine and manganese. The medicinal composition is mainly suitable for the crowd with hyperglycemia, effectively reduces the blood sugar, and can be applied for long time or applied according to course of treatment.
CN102617578A Imidazole derivative and medicine application thereof The invention relates to an imidazole derivative and a medicine application thereof, which discloses a compound of formula (1). Deifications of all variable groups are described in a description. The imidazole derivative and the medicine application thereof also relate to a method that the compound of the formula (1) is used for decreasing cell factors (such as TNF alpha or IL-1 beta) in the individual. The imidazole derivative and the medicine application thereof also relate to a method that the compound of the formula (1) is used for curing mediated diseases due to the fact that cell factors overgrow.
CN101905015A Medicine capable of decomposing alcohol, preventing drunkenness and protecting liver The invention relates to a medicine for protecting the liver, in particular to a medicine capable of decomposing alcohol, preventing drunkenness and protecting the liver, which can relieve the body pain of the people who drink and protect the body health, aiming at solving the problem of the injury of the alcohol for human body, avoiding liver injury and preventing and treating fatty liver and alcoholic liver. The medicine is prepared by the raw materials comprising the root of kudzu vine, radix paeoniae alba, liquorice, orange peel oil, plantain seed, fructus amomi, histidine, arginine, cysteine, glycin, glutamine, proteolytic peptide powder, fumaric acid, malic acid, vitamin C, vitamin E and zinc. Due to the action mechanism which is completely different from other dealcoholic drugs, the medicine does not hurt the liver when being used for antialcoholism, and effectively protects the liver.
US20100305043 Ccl18 and ccl3 methods and compositions for detecting and treating cancer The invention relates to methods of treating cancer by administering one or more chemokines that are downregulated in cancerous cells. More specifically, the invention provides methods for treating or preventing cancers such as malignant melanoma by administering a chemokine such as CCL18 and/or CCL3. The invention further provides methods for diagnosing cancer such as melanoma.
US20090291988 Reversible Inhibitors of Monoamine Oxidase A and B The instant invention relates to compounds of formula I, diagrammed below, wherein R3, E, D and Y are defined in the application, which are useful as reversible inhibitors of monoamine oxidase-B and/or monoamine oxidase-A, and therefore useful to treat or prevent neurological diseases or conditions in mammals, preferably humans.
CN103638563A Biological liquid of biological albumin glue The invention discloses biological liquid of biological albumin glue, which comprises the following components in parts by weight: 90-100 parts of sodium alginate, 80-110 parts of chitosan, 5-100 parts of edible starch, 5-100 parts of Kabo and 1,000-1,500 parts of water. By use of the organisms with functions of clearing heat and removing toxin, excreting water and diminishing swelling, stopping bleeding, promoting healing and preventing adhesion and by being matched with some biological formulas, the biological liquid disclosed by the invention can realize the functions of sterilizing, quickly stopping bleeding, promoting healing, preventing adhesion and diminishing inflammation, and realizes perfect curative effects on stopping bleeding and promoting healing after surgical treatment using biological albumin glue.
US20060127349 Administering water soluble complex of hypericin and a polyvinylpyrrolidone; diagnosing and treating tumors The invention relates to an active agent combination for diagnosing and treating tumours, comprising a water-soluble complex or a water-soluble compound of pure hypericin and a poly-N-vinylamide, especially PVP.
US7348354 Cyclohexylurea compounds Cyclohexylurea compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and the use of such compounds as pharmaceutically active agents with nociceptin/ORL1 receptor system activity for treating pain or other conditions associated with the nociceptin/ORL1 receptor system.
US20080221220 Antiinflammatory, antitumor and anticarcinogenic agents; rheumatic arthritis, psoriasis, transplant rejection, osteoporosis, Paget's disease, osteoarthritis, ankylosing spondylitis; 2',4'-dichloro-biphenyl-4-ylhydroxy or imine compounds The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 2′,4′-dichloro-biphenyl-4-yl-hydroxy-ketones and related compounds (collectively referred to herein as “DCBP compounds”), and more particularly to compounds selected from compounds of the following formula and pharmaceutically acceptable salts, solvates, and hydrates thereof: wherein: n is independently 1, 2, 3, or 4; W is independently —C(═O)—, —CH(OH)—, or —C(═NOROX)—; ROX is independently —H or C1-3alkyl; J is independently: —H, —RE1, —C(═O)—RE2, —C(═O)—O—RE3, —C(═O)—O—S(═O)2ORE4, —C(═O)—(CH2)n—C(═O)ORE5, —C(═O)—(CH2)n—NRNE1RNE2, —C(═O)—(CH2)n—NRNE3—C(═O)RE6, —C(═O)—(CH2)n—C(═O)—NRNE4RNE5, or —P(═O)(ORE7)(ORE8); wherein each of RE1, RE2, RE3, RE4, RE5, RE6, and RE7 is independently: —H, C1-3alkyl, -Ph, or —CH2-Ph. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment and/or prevention, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of, inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activation in rheumatoid arthritis, osteoporosis, cancer associated bone disease, Paget's disease and the like.
WO2014134800A1 Treatment of cervical cancer and/or ovarian cancer using transcription factor modulator In certain embodiments, the invention relates to a method of treating cervical cancer and/or ovarian cancer by administering a therapeutically effective amount of one or more transcription factor modulators disclosed herein, or a pharmaceutical composition thereof.
CN102688489A Pharmaceutical composition containing triptolide, triptolide derivative and Bc1-2 inhibitor and application thereof The invention relates to a pharmaceutical composition containing triptolide, triptolide derivatives and a Bc1-2 inhibitor, and its applications in preparation of medicaments for treating colon cancer, liver cancer, lung cancer, kidney cancer, stomach cancer, brain tumor, sarcoma, neuroglioma, pancreatic cancer, ovarian cancer, breast cancer, or prostate cancer. The pharmaceutical composition of the invention has significant synergistic effect, can improve medicament curative effect, decrease administration dosage, and reduce the generation of side effect.
WO2009075691A1 Cb-1 modulating compounds and their use Disclosed herein is a compound of Formula (1). Also disclosed herein is a method o modulating the activity of a cannabinoid receptor using a compound of Formula (I). Furthermore, disclosed herein is a method of treating a disease or condition that would be alleviated, improved or prevented by administration of a compound that modulates a cannabinoid receptor comprising identifying a subject in need thereof and administering to said subject a therapeutically effective amount of a compound of Formula (I). Also disclosed herein are pharmaceutical compositions comprising a compound of Formula (I).
CN101269041A Dexibuprofen sustained-release dropping pill and preparation method thereof The invention discloses a pharmaceutical preparation used for resisting inflammation, alleviating pain and eliminating fever, and particularly relates to a prepared sustained-release oral formulation adopting dexibuprofen as the ingredient. The pharmaceutical preparation aims to supplement the deficiency of the prior art and provide a sustained-release dexibuprofen dropping pill. The sustained-release dexibuprofen dropping pill overcomes the defects in the prior art effectively, guarantees no occurrence of an obvious quality change for the drug during the effective storage period and has the advantages of controllable release time, full release and high bioavailability simultaneously.
CN101502611B Medicament for treating cancer and preparation method thereof The invention relates to a drug for treating cancer and a preparation method thereof, belonging to the technical field of the drug and the preparation method thereof. The drug is characterized by comprising the following raw materials: 10000 portions of white wine matched with 8 to 12 portions of musk, 10 to 20 portions of capillary wormwood herb, 10 to 20 portions of artemisia princeps and prepared common monkshood daughter root, 10 to 20 portions of manchurian wildginger, 10 to 20 portions of cochinchina momordica seed, 10 to 20 portions of kusnezoff monkshood root, 15 to 25 portions of realgar,15 to 25 portions of ginseng, 1800 to 2200 portions of ophiorrhiza pumila, 800 to 1200 portions of barbed skullcap herb, 250 to 350 portions of Chinese toon root and 1800 to 2200 portions of garlic. The preparation method comprises the following steps of: 1) matching 10000 portions of white wine with 1800 to 2200 portions of garlic and soaking for 10 to 15 months; 2) screening, drying, weighing and disinfecting the ingredients of the drug, grinding realgar into fine powder, putting the obtained mixture in the white wine obtained from the step 1 according to required matching ratio for 10 to 20 days; 3) weighing musk according to matching ratio and grinding the musk into powder for future use; and 4) taking 500 portions of medicated liquor obtained from the step 2) to be matched with 0.3 to 0.8 portion of musk powder, mixing evenly and taking. The drug has good effect for treating cancer in early stage and middle stage, and preventing cancer; and the curative rate of the cancer in early stage is more than 90 percent.
US20120171158 METHODS OF USING sIP-10, CD26 INHIBITORS AND CXCR3 LEVELS IN A SAMPLE TO ASSESS CLEARANCE OF INFECTION, RESPONSE TO INTERFERON THERAPY, AND TREATING CHRONIC INFECTIONS The present invention relates to methods for the treatment of infection, a disease, or a condition using CD26 (DPIV) inhibitors. The present invention also relates to an antibody that binds to the IP-10 protein and a method of monitoring the necessity for administering a CD26 inhibitor to a patient, comprising evaluating a level of sIP-10, a activity of CD26, and/or a level of CXCR3 cells in a sample.
WO2005054251A1 New cartharidic amine, demethyl cartharidic amine derivatives and their medicinal use The invention relates to new cartharidic amine and demethyl cartharidic amine derivatives (I), and their intermediates (II), wherein P is glycol oligomer or amido acid oligomer, and the conjugates (III) of demethyl cartharidic amine derivatives (I) and polyglycol. Cartharidic amine and demethyl cartharidic amine derivatives (I), their intermediates (II), and the conjugates (III) have improved water solubility, less toxicity and side effect, inhibit enhanced activity of anti-cancer.
EP2183225A1 Cyclic amine substituted pyrimidinediamines as pkc inhibitors The invention encompasses Pyrimidine compounds and the compositions and methods using these compounds in the treatment of conditions in which inhibition of PKC and PKD is therapeutically useful.
CN101307076A Prodrug with liver-targeted anti-HBV effect The invention provides a prodrug of a hepatitis b virus resistant drug with a liver targeting action and a preparation method for the same. The prodrug is a prodrug of Adefovir or Tenofovir. Higher fatty acid, glyceride, cholic acid compounds or the base groups of derivatives thereof with the liver targeting action are connected with Adefovir or Tenofovir to prepare the prodrug. After being taken into a human body, the prodrug is concentrated in the liver and then is decomposed, thereby having the effects of reducing the dosage, improving the curative effect, reducing the drug concentration in a kidney and reducing the toxic and side effect. The invention also provides a method for synthesizing the prodrug.
WO2007075119A1 Pharmaceutical composition for photodynamic therapy and a method for treating oncological diseases by using said composition The invention relates to medicine, in particular to oncology and makes it possible to produce a pharmaceutical composition which is used for photodynamically treating malignant tumors and contains a therapeutically efficient substance of at least one type of fullerene C60 derivative selected from a group comprising a compound, in which a fullerene C60 molecule is covalently bound with an aminoacid or dipeptide molecule, or the pharmaceutically derivative thereof, or the complex of a compound with bio-compatible synthetic polymers or biopolymers and tetrapyrroles, or a conjugant of the compound with an aminocompound. Said accumulated in cells and photo-irradiated compounds convert a molecular oxygen into a singlet oxygen, generate free radicals and initiate biological processes for inhibiting the activity of tumor cells. A method for photodynamically treating malignant tumors using the inventive composition in the form of a photosensitiser is also disclosed.
EP2196460A1 Sulfonic acid salt compound of 4-carbamoyl-5-hydroxy-imidazole derivative The object is to provide a stable SM-108 derivative, which is effective as a carcinostatic agent, particularly an SM-108 derivative having good storage stability. An SM-108 compound having good storage stability can be produced by producing an organic sulfonic acid salt compound of SM-108. Further, a crystalline SM-108 compound containing a trace amount of an organic carboxylic acid can be produced by using an aqueous solution of the organic sulfonic acid salt of SM-108, and by adding an alkali metal salt of an organic carboxylic acid to the aqueous solution to neutralize the aqueous solution and then causing the crystal precipitation in the solution.
CN103417492A Olanzapine-containing biodegradable microsphere preparation and preparation method thereof The invention discloses an olanzapine-containing biodegradable microsphere preparation and a preparation method thereof. The olanzapine-containing biodegradable microsphere preparation comprises 10-50wt% of olanzapine or its salt, 0.5-20wt% of release adjusting agents and 30-89.5% of PLGA. In the invention, the PLGA having a proper monomer LA:GA ratio is selected as a matrix material, and above one release adjusting agents are added, so the olanzapine loading is improved to above 30%, and the particle size distribution and the in-vitro drug release of microspheres are improved. The utilization of a biodegradable material to encapsulate olanzapine to prepare the microspheres realizes a good slow release effect and the maintenance of an in-vivo relatively-stable drug concentration for above 15-45d or more.
WO2004098620A8 Activated carbon infusion solution, preparation method therefor and use thereof for the manufacture of drug for treating cancer The invention discloses activated carbon infusion solution, preparation method therefor and use thereof for the manufacture of drug for treating cancer. The said activated carbon infusion solution contains pure activated carbon microparticles injection solution, activated activated carbon microparticles injection solution, activated carbon injection solution adsorbing catalyst and various injection solutions carrying drugs, all of which are for intravenous use. It characterizes that the surface area of material activated carbon used is greater than or equal to 400-10000M2/g or higher, heavy metal content is less than or equal to 0.1-10ppm, other dissoluble metal ion content is less than or equal to 0.1-10ppm, crozzle is less than 2%, total pore cubage is greater than 0.3-6cm2/g, 0.15% methylene blue adsorptive value is greater than 6-30, the diameter of the activated carbon microparticles contained in this activated carbon infusion solution are ranged from 35 μ m to 2nm, the diameters are mainly ranged from 6 μ m to 2nm, in which 99% are ranged from 3 u m to 2nm, the microparticles which diameters are 6 μ m to 3 u m are not more than 1 %, the microparticles which greatest diameter is 35 μ m to 6 μ m have not more than 2 x 104 /mg activated carbon micropowder. When this activated carbon microparticles are intravenously injected into blood, they have good compatibility with tissues, have no toxicity or side effect, have no harmful stimulation, have no immunogenicity, they are safe and effective. They have incredible curative effect in treating cancer, blood vessels atherosclerosis, coronary heart disease, cerebral thrombosis, infectious diseases, azotemia, acute organic and inorganic poison poisoning.
US20060100171 Branched alpha-glucans for weight management Highly branched α-glucan having an average molar weight of at least 105 Da can be used for inducing or enhancing satiety and/or satiation in humans or animals by incorporation of the α-glucan into a liquid nutritional or pharmaceutical composition, preferably together with a food protein. The α-glucan induces a viscosity increase upon lowering the pH. The degree of branching of the α-glucan is at least 8%. Such α-glucans can be obtained e.g. by fermentation of lactobacillus strains having glucosyltransferase activity on a sucrose substrate.
US20050131026 Bronchitis; chronic obstructive pulmonary disease; antihistamines; pneumonia The invention relates to the use of proton pump inhibitors in the treatment of airway disorders.
EP1150686B1 Directly compressible matrix for controlled release of single daily doses of clarithromycin The invention refers to an improved pharmaceutical formulation for controlled release of clarithromycin or its derivatives, enabled by a novel combined matrix consisting of a fatty and a hydrophilic component, whereto also a surfactant and a pH-modulator may be added when an additional influence on the release profile of the active substance is desired.
US20080247953 Drug screening assays; SH2 docking domains; signal sequences; immunology; cyclophilins The present invention relates to drug screening assays, therapeutic protocols and pharmaceutical compositions designed to target non-receptor tyrosine family kinases and components of the tyrosine kinase family signal transduction pathways. This includes primarily diseases or conditions associated with immune responses and can include treatment for cancers as well as various immune disorders. The invention reports a novel substrate SH2 domain docking mechanism apart from the kinase active site that is required for appropriate tyrosine phosphorylation by these tyrosine kinases.
CN101708337B Preparation method of human serum albumin nano granules coated with oxaliplatin The invention relates to human serum albumin nano granules coated with oxaliplatin and a preparation method. The human serum albumin nano granules comprise oxaliplatin bulk pharmaceutical chemicals and human serum albumin HSA; in a preparation process, water for injection, anhydrous alcohol, glutaric dialdehyde and sodium hydroxide are used; the mass ratio of the oxaliplatin bulk pharmaceutical chemicals to the albumin is 10-25%, the concentration of an albumin water solution is 1-2.5% (g/ml), and the volume ratio of a precipitator of the anhydrous alcohol to the albumin water solution is 2:1-3:1; and the amino mole ratio of a cross-linking agent of the glutaric dialdehyde to the albumin is 75-200%, and the quantity of the sodium hydroxide is proper. The preparation method of the human serum albumin nano granules comprises the following five steps of directly carrying a medicine and removing a solvent, adsorbing the carried medicine and crosslinking, evaporating in a rotary way, precipitating in a centrifugal way and freeze-drying. The invention has the following advantages: (1) the anti-tumour efficacy of the oxaliplatin is retained, the limitation of quick metabolism of the oxaliplatin is changed, and the slow-release property of the medicine is enhanced; (2) the human serum albumin is used as a framework material, the compatibility of a human body is good, the humanserum albumin nano granules are safe and innoxious and can be biodegradable, and the concentration of a lymph circulation medicine can be increased.
CN101778947A nutritional compositions The present invention is directed to a novel saccharide composition isolated from a yeast culture. The invention is also directed to yeast cell based saccharide composition with increased water-solubility. The saccharide compositions disclosed in the invention can be used as nutritional or pharmaceutical additives or as part of nutritional or pharmaceutical composition in order to promote the health of an animal or human subject to which said composition is administered. The invention is also directed to methods of producing said saccharide compositions.
WO2014095833A1 Combination comprising radium-223 for the treatment of cancer The present invention relates to combinations comprising compounds A and B, compound A being a 17α-hydroxylase/C17,20-lyase (CYP17) inhibitor, and compound B being a pharmaceutically acceptable salt of the alkaline-earth radionuclide radium-223 and their use for the treatment or prophylaxis of a disease, particularly for the treatment of cancer.
EP1140909B1 Novel inhibitors of farnesyl-protein transferase Novel compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl-protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel aminooxyamide compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
WO2006076854A1 Combination medication for malignant tumors and application The invention relates to a method for treating malignant tumor by combination medication, and an anticancer medicinal composition with low poison and pharmaceutical preparation thereof . he composition which be used to treating malignant tumor is composed of the medicine which can increase the concentration of cAMP in cells and carboxyamidotriazole or its derivative or intermediate. According to the experimental result, such medicinal composition can increase cAMP levels in cells of adenylate cyclase activator forskolin, phosphodiesterase inhibitor theocin or IBMX, and can co-increase the depression effect of carboxyamidotriazole which can inhibit the cell proliferation of SH-SY5, Bel-7402 and Hela, so the medicinal composition can be used as broad-spectrum anti-malignant tumor medicine.
US7074574 Method of detecting growth differentiation factor-7 (GDF-7) using GDF-7 antibodies The present invention provides methods of using antibodies that bind to the growth differentiation factor-7 to identify GDF-7 in a sample.
US20110070253 Tumour-associated peptides binding to mhc molecules The invention relates to a tumour-associated peptide with an amino acid sequence that is selected from the group consisting of SEQ ID NO: 1 to SEQ ID NO: 101 of the attached sequence protocol, wherein the peptide has the ability to bind to a molecule of the human major-histocompatibility-complex (MHC) class-I. In addition, the invention relates to the use of the peptides and the nucleic acids encoding for the peptides for the production of a medicament, and for the treatment of tumorous diseases and/or adenomatous diseases. Furthermore, a pharmaceutical composition is described that has at least one of the peptides.
US20080096848 Substituted N-Aryl-9-Oxo-9H-Fluorene-1-Carboxamides and Analogs as Activators of Caspases and Inducers of Apoptosis The present invention is directed to substituted N-aryl-9-oxo-9H-fluorene-1-carboxamides and analogs thereof, represented by the general Formula I: (I) wherein R1-R8, X and Ar are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
CN101724934B Medicinal fibre used for treating cutaneous inflammation and pain, preparation and application thereof The invention relates to medicinal fibre used for treating cutaneous inflammation and pain, which comprises the components of cellulose acetate nano fibre, a ketoprofen ester precursor medicine and a medicinal percutaneous sorbefacient, wherein the ketoprofen ester precursor medicine accounts for 0.1-30% of the total weight of the fibre, the medicinal percutaneous sorbefacient accounts for 0.1-10% of the total weight of the fibre, and the cellulose acetate nano fibre accounts for 1-99% of the total weight of the fibre; the preparation of the medicinal fibre comprises the following steps: dissolving the ketoprofen ester precursor medicine, the medicinal percutaneous sorbefacient and the cellulose acetate into an organic solvent to prepare spinning liquid and then spinning to prepare the required medicinal fibre. The medicinal fibre has the effect of treating cutaneous inflammation and pain, has simple preparation method, convenient source of the raw materials and low cost, is friendly to the environment and is suitable for industrialized production; the fibre can be prepared into medicine-carrying clothings or other fabrics which directly contact with the skin of a human body, and the percutaneous administration is safe and comfortable.
CN102525939A Para-aminosalicylic acid sustained-release pellet with high drug-loading rate and enteric-coated preparation thereof The invention finds that the plasticity of a material can be enhanced and the problem of poor forming property of a pellet with a high drug-loading rate is solved when a highly-hydrophilic material generally serving as a disintegrating agent in a medicament is used for preparing a sustained-release pellet with high drug-loading rate. In the invention, an applicable highly-hydrophilic material is screened by breaking free from convention, reasonable using amount is researched, the contradiction between sustained release and disintegration of a medicament is avoided, a high-quality pellet is prepared, and a preparation has a sustained release function simultaneously. The invention provides a formula of a para-aminosalicylic acid sustained-release pellet with high drug-loading rate and a preparation process thereof, and provides an enteric-coated oral preparation prepared from the sustained-release pellet.
EP2068881A2 Method of treating thermoregulatory disfunction with paroxetine The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature.
CN1947720A Clarithromycin liposome microsphere injection and its prepn. method A lipide microball type injection of clarithromycin with high stability and low toxin is prepared from the oil for injection, clarithromycin, surfactant, glycerin, oil-phase solubilizer, metallic chelating agent, and the water for injection. Its preparing process is also disclosed.
CN1679621A Medicine for treating colpitis A medicine in the form of capsule for treating vaginitis is prepared from povidone iodine and pharmacologically acceptable auxiliaries.
US7786311 1,2,4-thiadiazolium derivatives as melanocortin receptor modulators The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.
US20120083513 3-Substituted-8-Substituted-3H-Imidazo[5,1-d][1,2,3,5]tetrazin-4-one Compounds and Their Use The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and —B are as defined herein (collectively referred to herein as 38TM compounds): The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
US7087618 Pyrazolopyridinyl pyrimidine therapeutic compounds The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents
EP0931078B1 Novel tricyclic piperidinyl compounds useful as inhibitors of farnesyl-protein transferase Novel tricyclic compounds of formula (1.0) or a pharmaceutically acceptable salt or solvate thereof, wherein: one of a, b, c, and d represents N or NR9, wherein R9 is O-, -CH¿3? or -(CH2)nCO2H wherein n is 1 to 3, and the remaining a, b, c and d groups represent CR?1 or CR2¿; or each of a, b, c and d is independently selected from CR?1 or CR2¿; each R1 and each R2 is independently selected from H, halo, -CR¿3?, -OR?10, -COR10, -SR10¿, -S(O)¿tR?11 (wherein t is 0, 1 or 2), -SCN, -N(R10)2, -NR?10R11, -NO¿2, -OC(O)R10, -CO2R10, -OCO¿2R?11, -CN, -NHC(O)R10, -NHSO¿2R?10, -CONHR10, -CONHCH¿2?CH2OH, -NR?10COOR11, -SR11C(O)OR11, -SR11N(R75)2¿; n is 0 (zero), 1, 2, 3, 4, 5 or 6; T is -CO-; -SO-; -SO¿2?-; or -CR?30R31¿-; Z represents alkyl, aryl, aralkyl, heteroalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -OR?40, -SR40, -CR40R42, -NR40R42¿, formulae (i), (ii), (iii), (iv), (v) and (vi). Pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
US20100135954 6-Phenylpyrimidinones as PIM Modulators A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
EP0938900B1 Preventives/remedies for stomatitis Preventives/remedies for stomatitis containing L-zinc carnosinate salt or L-carnosin/zinc complex optionally together with sodium alginate. These drugs are excellent in the effects of treating and preventing stomatitis, in particular, one caused by chemotherapy or radiation therapy for cancer.
CN101791397A Application of RNase III protein in staphylococcus aureus for preventing and treating staphylococcus aureus infection The invention belongs to the technical field of biology and relates to the application of staphylococcus aureus RNase III protein. As a ribonuclease in the staphylococcus aureus, the RNase III protein participates in synthesis and secretion of staphylococcus aureus exocrine protein, thereby affecting the pathogenicity of the staphylococcus aureus. Thus, the RNase III protein has good application prospect in the field of preventing and treating staphylococcus aureus infection.
WO2008134513A3 Copper lowering treatment of autoimmune diseases The present invention relates generally to the field of prophylaxis and therapy for autoimmune diseases. In particular, the present invention is related to agents that can bind or complex copper, and to the use of these agents in the prevention and/or treatment of autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosis, and multiple sclerosis.
US20100323952 Nucleoside Analogs in Combination Therapy of Herpes Simplex Infections A pharmaceutical product comprising a nucleoside analogue active against herpes simplex virus, such as acyclovir/valaciclovir or peniclovir/famciclovir, and an immunosuppressant, as a combined preparation for simultaneous, separate or sequential use in the treatment and/or prevention of herpes simplex virus infections.
CN101156865B Antineoplastic new usage of cardiac glycoside compound in antiar The invention relates to the medicine technology field, in particular relates to a new application of cardiac glycoside chemical compound having general formula (I) in preparing oncotherapy drug, wherein, R equals to 2-O-methyl-Beta-D-mycose, 6-deoxidation-Beta-D-gulose or 6-deoxidation-2-O-methyl-Beta-D-allose. The cardiac glycoside chemical compound can be obtained through a separation from upasin various conventional separation methods or be obtained through a synthesis or semisynthesis method.
WO2012159444A1 Acupoint injection An acupoint injection, the components whereof comprise a saturated solution of phenol at normal temperature and saline mixed at a ratio of 0.5 to 2 : 100. The injection employs phenol in the form of a saturated solution at normal temperature and diluted in the saline. The injection stimulates the original functions of an acupoint and enhances same, thereby improving the therapeutic effectiveness, and achieving the purpose of curing diseases.
CN102861064A Application of Houttuynoid E in medicine for treating laryngocarcinoma The invention discloses application of Houttuynoid E in preparation of a medicine for treating laryngocarcinoma, belonging to the technical field of new application of medicine. The invention discovers that Houttuynoid E has the remarkable inhibitory effects on the growth of human laryngocarcinoma cell strains including HEP-2, TU686, M2e and M4e through the evaluation of in vitro MTT antineoplastic activity. Therefore, Houttuynoid E can be used for preparing the anti-laryngocarcinoma medicine and has good development and application prospects. The application of Houttuynoid E in preparation of the medicine for treating laryngocarcinoma provided by the invention is disclosed firstly, the skeleton type belongs to new skeleton type, and the inhibitory activity of Houttuynoid E on laryngocarcinoma cells is unexpectedly strong.
US20120136027 Phenyl Ethynyl Derivatives As Hepatitis C Virus Inhibitors Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R* have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in the treatment or prophylaxis of HCV.
CN102048715B Applications of trans-acomhole in preparing medicine or health care products The invention discloses a new effect and applications of trans-acomhole, relating to three new applications of the trans-acomhole in preparation of drugs or health care products for preventing and treating enterocoelia adhesion after an enterocoelia operation, abdominal distension as well as functional gastrointestinal disorder and poor digestion and malabsorption. By intervening the trans-acomhole through an animal model and a clinic test by the applicant, the trans-acomhole is proved to be capable of being used as the drugs or health care products for preventing and treating the enterocoelia adhesion after the enterocoelia operation, the abdominal distension as well as the functional gastrointestinal disorder and poor digestion and malabsorption. The drugs or health care products can bepreparations for external application, oral preparations or intraperitoneal injection preparations.
WO2010033198A3 Analogs of indole-3-carbinol and their use as agents against infection Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2'-diindolylmethane, 2',3-diindolylmethane, and 3,3'-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
CN101440096A 1-(3',4',5'- trisubstituted phenyl)- tetrahydroisoquinoline compound and its use The invention relates to a 1-(3', 4', 5'-trisubstituted phenyl)-isoquinolin compound with tumor cytotoxicity shown in a formula (1) and intermediate compounds thereof or pharmaceutical salts or solvates thereof, The invention also relates to a method for preparing the compounds in the formula (1), pharmaceutical compositions and medicinal application thereof. The compounds have certain activity of inhibiting growth of tumor cells, and can be expected to be used as anti-tumor drugs. A structural formula (1) of the invention is shown in a figure.
CN102357099A Pharmaceutical composition with ornidazole The invention provides an ornidazole composition and a preparation process thereof, and particularly relates to a mixture of ornidazole and borax; compared with drug with a single component, the composition of the invention has doubled curative effect and obviously shortened treatment period after the composition is used by patients.
CN101390849A Allitride composition and method thereof for preparing drop capable of treating nasal cavity microbial infection and use thereof The invention relates to a medicine for the treatment of microbial infection, in particular to allitridon drops used for the treatment of microbial infection. The allitridon drops mainly contain the following ingredients, 0.8-4ml of diallyl trisulfide, tween-80 with the amount of dissolving the diallyl trisulfide, 7-9g of NaCl, 1000ml of distilled water. The allitridon drops have the advantages of being applicable to the treatment of microbial infection, good treatment effects and low cost.
CN103005674A Albizia flower odor type snuff The invention belongs to the technical field of snuff products, relates to albizia flower odor type snuff made of purely natural raw materials, and further relates to a method for manufacturing the snuff. The snuff comprises, by weight, from 50 to 150 parts of flos magnoliae, from 10 to 90 parts of radix pseudostellariae, from 100 to 300 parts of mulberry leaves, from 0.1 to 0.4 part of borneol, from 0.03 to 0.10 part of asarum, from 0.01 to 0.09 part of rhinoceros horns, from 5 to 15 parts of grassleaf sweelflag rhizome, from 25 to 125 parts of tobacco leaves, from 2 to 6 parts of Chinese eaglewood, from 2 to 6 parts of flos caryophylli, from 5 to 25 parts of radix angelicae dahuricae, from 2 to 6 parts of menthol, from 0.05 to 0.35 part of musk, from 100 to 500 parts of tea leaves and from 50 to 150 parts of red wine. The snuff has faint scent of albizia flowers after the albizia flowers are smoked. Besides, the snuff can realize a refreshing effect and a nasal ventilation effect, and can assist in quitting smoking.
CN101514179A Indolone hydrazine ethylidene carbonyl compound, method for preparing same and application thereof in medicine The invention relates to an indolone hydrazine ethylidene carbonyl compound represented by a general formula (I) or a pharmaceutically accepted salt, hydrate or solvent compound thereof, a method for preparing the same and application thereof in medicine.
CN102327221A Cefadroxil liposome solid preparation The invention provides a cefadroxil liposome solid preparation. The cefadroxil liposome solid preparation consists of the following components in part by weight: 125 parts of cefadroxil, 90 to 120 parts of phosphatidylinositol, 30 to 40 parts of dimyristoyl phosphatidylcholine, 50 to 70 parts of cholesterol and 300 to 500 parts of other auxiliary materials which are used commonly and pharmaceutically. The liposome solid preparation is high in entrapment rate, and has uniform grain sizes, and medicines can be kept for a long time in blood circulation; and the quality of the preparation products is improved, the toxic and side effects are reduced, the equipment of a preparation method is simple and is easy to operate, and the cefadroxil liposome solid preparation is suitable for large-scaleindustrial production.
WO2011069921A1 Sucrose octasulfates of zinc, the preparation of same and the pharmaceutical and cosmetic uses thereof The present invention relates to an sucrose octasulfate of zinc of general formula (I), to the method for the preparation of same and to the use thereof in the pharmaceutical and/or cosmetic field, where: 0 ≤n ≤ 4, n is an integer, and Y is OH, CI, Br, I, NO3, C6H5O7, CH3CO2, CF3CO2 or -OCH3.
WO2008143677A1 Stable solid elsamitrucin salts suitable for pharmaceutical formulations Stable solid, crystalline forms of elsamitrucin salts are provided that are useful in preparing anti-neoplastic parenteral formulations. Also provided are methods for treating neoplastic diseases in humans using parenteral formulations that include at least one stable elsamitrucin salt.
EP2001483B1 Use of cholest-4-ene-3-one derivatives to obtain a cytoprotective medicine This invention relates to the use of cholest-4-in-3-one derivatives to obtain a cytoprotective medicine, excluding a neuroprotective medicine.
CN101293042B Medicament for treating necrosis of femoral head The invention discloses a drug for treating femoral head necrosis, which consists of nine raw materials that are danshen root, sanchi, himalayan teasel root, twotooth achyranthes root, membranous milkvetch root, yanhusuo, shinyleaf pricklyash root, prepared common monkshood mother root and calcined native copper, and the mix ratio by weight of the raw materials is as follows: 8 to 90 parts of danshen root, 7 to 80 parts of sanchi, 7 to 80 parts of himalayan teasel root, 7 to 80 parts of twotooth achyranthes root, 6 to 70 parts of membranous milkvetch root, 5 to 60 parts of yanhusuo, 4 to 50 parts of shinyleaf pricklyash root, 4 to 50 parts of prepared common monkshood mother root and 1 to 10 parts of calcined native copper. Compared with the prior art, the invention is characterized by significant efficacy, evident pharmacological effects, lower toxicity and side effects, convenient administration, appropriate price and so on, which further has the effects of activating blood circulation, removing blood stasis, activating qi-flowing, relieving pain, invigorating kidney and growing bone and can be used for treating the symptoms of femoral head necrosis and fractures.
CA2842566A1 Pyrazoline derivatives and their use as selective androgen receptor modulators The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I), in which the substituents are as defined in the specification; to compounds of formula (I) for use as androgen receptor modulators. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
EP2582368A1 Acetyl-carnitine for use in a method for increasing neurogenesis in neural tissue The invention described herein is directed to the use of acetyl L- carnitine, or propionyl L-carnitine, or a salt thereof, for preparing a medicament for increasing neurogenesis in neural tissue; in which said increased neurogenesis is useful for preventing central nervous system disorders due to ageing or genetic predisposition.
CN102349901A Application of pirfenidone in preparation of medicaments for controlling proliferative diseases after ophthalmologic operation and eye drops thereof The invention discloses an application of pirfenidone in the preparation of medicaments for controlling proliferative diseases after an ophthalmologic operation and eye drops thereof. According to the invention, pirfenidone is prepared into the eye drops. Experiments show that pirfenidone has good stability and good ocular tissue permeability, can inhibit HLECs migration and propagation, and has no cytotoxicity to HLECs within the action range (0-1mg/ml). With pirfenidone being within the range of 0-1%, the eye drops are continuously applied on eyes within a month with safety and with no obvious toxic and side effect. Pirfenidone can be used to delay the generation of PCO after the rabbit corneal Phaco operation, reduce HLECs propagation and minimize the shield of PCO to an optical region. In addition, there is no obvious ocular surface injury or postoperative inflammation aggravation and severe adverse reaction after PFD is applied in the rabbit corneal Phaco operation. Therefore, pirfenidone can be used to control proliferative diseases after an ophthalmologic operation, especially posterior capsule opacification generated after a cataract surgery.
WO2010076323A1 Use of ammonium chloride in therapy The present invention relates to a method for the pharmaceutical treatment of hepatic failure and necrosis, which is caused by various toxic agents, and for the treatment of viral infections or other diseases, specifically tumors, that can be treated with interferons. More particularly, the present invention relates to a method of treating or preventing a viral infection, hepatic failure, hepatic necrosis or other conditions caused by toxic agents or by autoimmune reaction or a tumor that is susceptible of treatment with interferons alfa, beta or gamma, the said method comprising administering a pharmaceutically effective amount of a NH4Cl dosage form together with pharmaceutically acceptable excipients to a patient in need thereof.
WO2012057300A1 Novel pyridine derivative The present invention provides a novel compound which comprises a compound represented by formula (I) [wherein X1, X2 and X3 are the same as or different from one another and independently represent a nitrogen atom, CH or the like; Y represents a single bond, -CH=CH- or the like; Z1 and Z2 are the same as or different from each other and independently represent CH, a nitrogen atom or the like; R1, R2 and R3 are the same as or different from one another and independently represent a hydrogen atom, a C1-6 alkyl group or the like; R4 represents a hydrogen atom, a C1-6 alkoxy group or the like; R5 represents an aryl group, a heteroaryl group or the like; R6, R7 and R8 are the same as or different from one another and independently represent a hydrogen atom, a C1-6 alkyl group or the like; and n represents an integer of 0-2] or a salt thereof, and which is useful as a therapeutic agent and/or a prophylactic agent for neuropsychiatric diseases associated with beta-amyloid.
WO2009119554A1 Promoter for bicarbonate secretion in gastrointestinal tract Disclosed is a substance which can prevent or treat a disease associated with the secretion of an acid. A calcium receptor activator is used as an active ingredient of a promoter for the bicarbonate secretion in a gastrointestinal tract. Examples of the calcium receptor activator include γ-Glu-X-Gly [wherein X represents an amino acid or an amino acid derivative], γ-Glu-Val-Y [wherein Y represents an amino acid or an amino acid derivative], γ-Glu-Ala, γ-Glu-Gly, γ-Glu-Cys, γ-Glu-Met, γ-Glu-Thr, γ-Glu-Val, γ-Glu-Orn, Asp-Gly, Cys-Gly, Cys-Met, Glu-Cys, Gly-Cys, Leu-Asp, γ-Glu-Met(O), γ-Glu-γ-Glu-Val, γ-Glu-Val-NH2, γ-Glu-Val-ol, γ-Glu-Ser, γ-Glu-Tau, γ-Glu-Cys(S-Me)(O), γ-Glu-Leu, γ-Glu-Ile, γ-Glu-t-Leu and γ-Glu-Cys(S-Me).
CN101732294A Anti-tumor application of tanshinone compound The invention relates to an application of a tanshinone compound in preparing anti-tumor medicaments, and the prepared medicaments can resist tumors, such as brain tumors, lung cancer, liver caner, breast cancer, prostatic cancer, pancreatic cancer, cervical cancer, gastric cancer, esophagus cancer, and the like. Proved by experiments, the tanshinone compound is concentration-dependent to suppress the proliferation of tumor cells. The compound can obviously induce the expression of quinone reductase and obviously suppress the generation of tumor vessels, thus the compound can also be used for preparing cancer chemical prevention medicaments, anti-inflammatory medicaments and medicaments for suppressing the generation of the tumor vessels. Frequently used low-price reagents, such as alcohol, chloroform, methanol, silica gel, and the like, are used for separating tanshinone compound monomers from medicinal materials. The method is simple and reliable, has low cost and high efficiency, can be used for carrying out industrialized mass production and is beneficial to popularization and application. The tanshinone compound has a structural general formula disclosed in the specification.
EP2270007A1 2-N-{5-[[4-[2-(methyl-2-pyridinylamino) ethoxy] phenyl]methyl]-2-4-thiazolidinedione} butanedioic acid, methods of preparation and compositions with rosiglitazone maleate The disclosure relates to a pharmaceutical composition comprising a granulate of a mixture of: a) rosiglitazone maleate; b) at least one pharmaceutically acceptable carrier; and c) less than 0.1% of the compound of the formula (I): based on the combined weight of the compound of the formula (I) and rosiglitazone maleate.
CN201515888U A dual purpose pillow for neck portion and waist portion The utility model relates to a dual purpose pillow for the neck portion and the waist portion, which comprises a pillow core, a pillow slip, and further a hard pillow seat. The body of the hard pillow seat is a hard strip shaped rectangular body. In use, the pillow core is put into the main slip of the pillow slip, and the pillow slip is wound around the hard pillow seat into a cylindrical pillow body, then the cylindrical pillow body is fixed by fixing pieces. The shape of the pillow slip is rectangular, and besides the main slip, a first laying slip is included on one end along the length direction thereof for laying the hard pillow seat, and a second laying slip is further included on one end along the width direction of the pillow slip for laying the hard pillow seat. And the pillow can be used for the waist in use. Because of the supporting function of the hard pillow seat, the utility model can ensure that the pillow body will not deform in the use process, thus has function of supporting the neck; the utility model can also be used to support the waist by changing the laying position of the hard pillow seat in use.
WO2013017073A1 Quinazoline derivative, composition having the derivative, and use of the derivative in preparing medicament As represented by Formula (I), a quinazoline derivative, or a pharmaceutically acceptable salt thereof, or a solvate thereof, a pharmaceutical composition having the compound or the pharmaceutically acceptable salt thereof or the solvate thereof, and a method for preparing the compound as represented by Formula (I). R1 is represented by Formula (II) or Formula (III), and R2 is represented by Formula (IV) or Formula (V), while the definitions of other substituent are as presented in the description. The compound represented by Formula (I) is provided with inhibitory activity with respect to one or several kinases among EGFR, VEGFR-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70, and fyn.
EP1539957A1 Novel diagnostic and therapeutic methods and reagents therefor This invention provides novel methods of detecting or treating aberrant cell cycle regulation associated with expression of a nuclear protein encoded by a gene that is linked to map position 8q22.3 of the human genome, and to novel reagents that are useful therefor. More particularly, the invention provides novel nucleic acid and proteinaceous probes, for detecting a gene that is linked to map position 8q22.3 of the human genome or the expression products thereof, wherein expression or elevated expression of said gene is associated with the appearance or occurrence of tumors associated with cancer, DNA damage and progesterone-receptor-mediated effects on cells. The invention also provides reagents and methods for detecting or modulating the expression products of the gene, such as, for example, in the diagnosis or treatment of cancer, cellular proliferation, DNA damage or progesterone receptor-mediated effects on cells.
US20120058079 1,2,5-Oxadiazoles as Inhibitors of Indoleamine 2,3-Dioxygenase The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
WO2014059284A1 Method of preparing resin tinctures Described herein are methods for making a pharmaceutical composition for topical, transdermal or transmucosal delivery of a pharmaceutically active agent comprising combining (i) a first composition comprising or consisting of a pharmaceutically active agent and, optionally, a first volatile solvent and/or water, and (ii) a second composition comprising a resin, a second volatile solvent and 10-40% v/v water. Compositions made by these methods also are described, as are compositions comprising a pharmaceutically active agent, a volatile solvent, a resin and 10-40% (w/v) water, and containers containing such compositions or components thereof.
US7312213 Substituted benzo[e][1,4]oxazino[3,2-g]isoindole compounds A compound selected from those of formula (I): wherein: W1, with the carbon atoms to which it is bonded, represents phenyl or pyridyl, Z represents a group selected from hydrogen, halogen, linear or branched (C1-C6)alkyl, aryl, aryl-(C1-C6)alkyl, aryloxy, aryl-(C1-C6)alkoxy, hydroxy and linear or branched (C1-C6)alkoxy, R1 is as defined in the description, R2 represents hydrogen or —CH2CH2O—R8, R3 and R4 each represents hydrogen, linear or branched (C1-C6)alkyl, aryl or aryl-(C1-C6)alkyl, n represents an integer of from 1 to 6 inclusive, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.
US20080255076 Steroid-Derived Pharmaceutical Compositions The present invention relates to the use of specific steroid derivatives in the preparation of medicaments for the treatment or prevention and/or amelioration of disorders relating to pathological processes in lipid rafts.
WO2009098612A3 Polymorphic form of a [1, 2, 4] triazolo [4, 3-a] pyridine derivative for treating inflammatory diseases The present invention relates to a polymorphic form B of Λ/-[3-tert-butyl-1-(3- chloro-4-hydroxyphenyl)-1 H-pyrazol-5-yl]-N-{2-[(3-{2-[(2-hydroxyethyl)sulfanyl] phenyl}[1,2.4]triazolo[4,3-a]pyridin-6-yl)sulfanyl]benzyl}urea (I) as defined herein. This polymorph is useful in the treatment of various conditions, particularly in the treatment of inflammatory conditions such as chronic obstructive pulmonary disease.
WO2013171317A1 Pyrazole derivatives and their use as lpar5 antagonists The present invention relates to compounds of the formula (I), wherein theresidues R1 to R5, V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in thetreatmentof diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.
US20060148829 Means for inducing differentiation of supernumerary hair cells and deiters' cells in the developing organ of corti Use of at least one kinase inhibitor for making drugs for inducing differentiation of supernumerary hair cells and Deiters' cells in the developing organ of Corti.
CN102204917A Pharmaceutical composition containing fasudil and sildenafil, and preparation method and application thereof The invention relates to a pharmaceutical composition containing fasudil and sildenafil for treating pulmonary hypertension, and a preparation method thereof, belonging to the field of pharmacy. The composition provided by the invention uses fasudil and sildenafil as the pharmaceutical active components, and the composition also comprises other pharmaceutically acceptable carriers, such as a disintegrant, an adhesive, an excipient, a thinner, a lubricant, a skeletal material for controlling the release rate of the active components in a sustained or controlled release preparation, and the like, and the suitable carriers are selected for different dosage forms.
WO2014082889A1 Novel imidazolines as dual inhibitors of mdm2 and mdmx Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, methods for making said compounds as well as methods of using them in the treatment of cancer.
WO2010120203A1 Use of organic dyes as analgesic agents The invention relates to the use of an organic dye selected from a group containing crystal violet, gentian violet, malachite green oxalate and rhodamine 6G as an analgesic agent in the form of a solution with the agent dosage ranging from 0.000001 mg to 10 g per administration. Preferably, the agent is administered at least twice a day. In particular cases of use the agent is perorally administered in the form of an aqueous solution before or after meals, or is rectally administered in the form of an aqueous solution, or a 1% solution of the agent is intravenously injected, or the agent is used in the form of a 1-5% ointment, or the agent is rectally administered in the form of suppositories, or, for managing cancer pain, the agent is injected into a tumor (under a tumor) or into a metastasis. The invention makes use of widely available, inexpensive, non-toxic, non-allergic and non-addictive substances, administered in pharmaceutically acceptable doses, and makes it possible to reduce treatment time, enhance treatment efficiency, provide pain relief without affecting the patient's functional capacity, use a minimum of analgesic agents of different activity and completely exclude the need for opiates.
WO2008006582A1 Compositions comprising magnolol or honokiol and other active agents for the treatment of inflammatory diseases The present invention relates to novel compositions comprising magnolol and/ or honokiol and at least one additional component e.g. selected from ligustilide, oleuropein (I), oleuropein aglycone (II), hydroxytyrosol, rosehip, genistein, resveratrol, EGCG, cashew fruit extract and Glycyrrhiza foetida as well as to the use of these compositions as a medicament, in particular as a medicament for the treatment, co-treatment or prevention of inflammatory disorders.
EP1453830B1 Pyrazolo-pyridine derivatives as antiherpes agents The present invention provides compounds of formula (I):Insert Formula (I) herewherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
US8318726 Benzylidineanthracenone linked pyrrolobenzodiazepine hybrids useful as anticancer agents and process for the preparation thereof The present invention provides a compound of formula 5, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of formula 5a-t.
CN102614135A Cytidine disodium triphosphate suspension powder injection and preparation method thereof The invention relates to novel preparation formulation of cytidine disodium triphosphate, in particular to cytidine disodium triphosphate suspension powder injection and a preparation method thereof. The powder-injection comprises the following components as per parts by weight: 1 part of cytidine disodium triphosphate, 0.1 to 10 parts of surface active agent and 2 to 15 parts of cryoprotectant. The powder injection improves the stability of cytidine disodium triphosphate, can be slowly administrated in body for a long time, and greatly improves the bioavailability. Protein of the surface active agent (stabilizing agent) is degraded in body, has no toxicity and immunogenicity, can effectively increase the pharmacological treatment index, and reduces the drug toxicity and the drug side-effect.
WO2007092978A1 Use of gallium(iii) complexes for the treatment of melanomas The invention relates to the use of gallium(III) complexes for the treatment of melanomas.
CN1919196A Slow release tablet comprising toraesmide active ingredient The invention discloses a slow release tablet containing active ingredient of torasemide, which comprises torasemide, slow release material and other auxiliary materials by the weight ratio of 1 : 0.2-20 : 10-200, preferably 1 : 0.5-10 : 20-100. The prepared slow release tablet is suitable for patients of hypertension.
WO2009018367A3 Salt forms of (2s)-(4e)-n-methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine Salts of (2S)-(4E)-N-methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine, methods for their preparation, pharmaceutical compositions comprising said salts, and their use are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat or prevent such disorders.
US20140088127 Novel process to prepare pioglitazone via several novel intermediates A novel process for preparing thiazolidinediones, preferably Pioglitazone, as described. Also described are novel intermediates involved in its synthesis and process for their preparation and use in medicine.
CN103446044A Liranaftate ointment and preparation method thereof The invention discloses a liranaftate ointment and a preparation method thereof. The ointment is prepared from an inner oil phase, an outer oil phase and a water phase, wherein the inner oil phase is composed of liranaftate and poloxamer 124; the outer oil phase is glycerin monostearate meltwater; the water phase is composed of isopropanol, water, and a preservative. The ointment disclosed by the invention has the advantages of uniform drug dispersion, uniform content and stable quality, therefore, the liranaftate ointment is beneficial for long-term storage and transportation.
CN101536985A Livestock cefquinome lung-targeted microspheres and preparation method thereof The invention belongs to the technical field of veterinary drugs. The invention discloses a veterinary drug of cefquinome microspheres serving as a lung-targeted preparation prepared by using cefquinome as a raw material and a preparation method thereof. The cefquinome is used as the raw material and gelatin is used as a carrier to form micropheres, and the ratio of the cefquinome to the gelatin is 1:2. The preparation method comprises the following steps: firstly, dissolving the cefquinome in a solution of the gelatin, uniformly mixing the cefquinome and the solution of the gelatin; secondly, dripping the mixed solution in sorbitanmonooleate and liquid paraffin and uniformly stirring the mixture till the mixture turns milky white; quickly cooling the mixture to below 5 DEG C in an ice bath, adding glutaric dialdehyde in form of thin flow, and continuing stirring for cross linking and curing; dehydrating the product obtained with isopropanol, and performing stirring and suction filtration; and washing the dehydrated product with a small amount of isopropanol and ether to remove the glutaric dialdehyde completely, washing away the liquid paraffin on the surface of the microspheres with petroleum ether and drying the microspheres at room temperature and under vacuum to obtain the cefquinome microspheres. The preparation effectively improves tissue selectivity of drug, slows drug release, improves treatment effect, reduces toxic and side effects, and achieves slow release, long-lasting effect and targeting.
WO2013068489A1 Heterocyclic carboxamides useful as inhibitors of phosphodiesterase type 10a Novel inhibitor compounds of phosphodiesterase type 10A The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
WO2007080902A1 Composition inhibiting the expression of target gene in eyeball and remedy for disease in eyeball It is intended to provide a composition which contains a liposome having an RNA enclosed therein, wherein the RNA contains a sequence consisting of 15 to 30 consecutive bases in mRNA of a target gene relating to a disease in the eyeball and a sequence complementary to the above-described sequence, and by which the liposome reaches to the eyeball. The liposome having the RNA enclosed therein is a liposome comprising, for example, a complex particle composed of a lead particle containing a cationic lipid and a particle having the RNA as the constituents thereof and a bimolecular lipid membrane coating the complex particle. The bimolecular lipid membrane is a bimolecular lipid membrane having a neutral lipid, a lipid derivative of a water-soluble substance, a fatty acid derivative or an aliphatic hydrocarbon derivative as the constituents.
US20100173825 Heteroaryl benzamide derivatives The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, R2, R3, n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).
US20080226597 Viricidal protein for prevention and treatment of hepatitis infection The present invention provides evolved interferon-alpha polypeptides, and conjugates thereof, and nucleic acids encoding the polypeptides. The invention also includes compositions comprising these polypeptides, conjugates, and nucleic acids; cells containing or expressing the polypeptides, conjugates, and nucleic acids; methods of making the polypeptides, conjugates, and nucleic acids; and methods of using the polypeptides, conjugates, and nucleic acids.
EP1220661B1 Transdermal therapeutic system for administering acetylsalicylic acid and/or salicylic acid The invention relates to a transdermal, therapeutic system in the form of a plaster which contains acetylsalicylic acid and/or salicylic acid. Said system has a backing layer, an active ingredient reservoir attached thereto, a membrane which controls the administration of the active ingredient in the absence of other control mechanisms, an adhesive device for fixing the system onto the skin and a protective layer which can be detached before application. The system is characterised in that it contains at least one component from the group of pyrrol derivatives and at least one component from the group of terpenes.
CA2427340C Cyp1b1 nucleic acids and methods of use The present invention provides nucleic acids containing transcriptional units that encode CYP1B1 polypeptides or portions thereof, wherein the transcriptional units lack sequences found in the untranslated region (UTR) of naturally occurring forms of the CYP1B1 transcript. Then nucleic acids of the invention lack translational repressor elements and thus provide for a system of enhanced translation of the CYP1B1 polypeptide or portions thereof. Also disclosed are methods of administering nucleic acids to a mammal and use in the treatment of proliferative disorders or cancer.
US20130029931 Pleurotus tuber-regium polysaccharide functionalized nano-selenium hydrosol with anti-tumor activity and preparation method thereof The preparation of Pleurotus tuber-regium polysaccharide functionalized nano-selenium hydrosol with anti-tumor activity includes the following steps: 1) at normal temperature and under normal pressure, adding a Vitamin C solution to an aqueous solution of Pleurotus tuber-regium polysaccharides, and mixing uniformly; 2) adding dropwise a selenium dioxide solution or a selenite solution to the solution while mixing uniformly; and 3) adding water to the solution to a pre-determined volume, to obtain a Pleurotus tuber-regium polysaccharide functionalized nano-selenium hydrosol when the red color of the product is no longer deepened. The polysaccharides are used to control the particle size of nano-selenium, to obtain functionalized nano-elemental selenium with high anti-tumor activity and low toxicity. The anti-tumor activity of the biologically active molecule polysaccharides and the physiological effect of nano-selenium are combined, and a synergistic anti-tumor effect is achieved.
CN103479663A Application of yeast-origin glucan on preparation of drugs for curing hepatitis B virus infection The invention belongs to the field of medicine, relates to an application of yeast-origin glucan on preparation of drugs for curing hepatitis B virus infection, and especially relates to an application on preparation of drugs for reducing or eliminating serum surface antigen of chronic hepatitis B virus infected patients. It has been testified by tests that the yeast-origin glucan can modulate the cell factor expression of mice spleen cells, increases the expressions of IL-12, IL-1, and TNF, and decreases the expression of inhibiting cell factor IL-10; can promote the maturity of mDC of HBV C57BL/6J-TgN transgenic mice, and increases the expressions of mDC surface co-stimulatory molecules CD80 and CD 86; is capable of prominently strengthening the generation of peripheral blood-derived PBMC IFN-gamma of HBV infected patients. The yeast-origin glucan can be used for preparation of drugs for curing hepatitis B infection, especially preparations of drugs for reducing or eliminating serum surface antigen of chronic hepatitis B virus infected patients, and can be taken as an immunity strengthening agent to help the treatment of HBV infection.
US20130004428 Diazabicyclononyl oxadiazole compounds and their use as nicotinic acetylcholine receptor modulators This invention relates to diazabicyclononyl oxadiazolyl derivatives, which are found to-be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Ar1 represents a pyrrolyl group, optionally substituted with alkyl or halo-alkyl.
WO2014071438A1 Modified polyphenols and modified polyphenol compositions This invention relates to polyphenolic compounds, in particular ethoxylated polyphenolic compounds and the use of such compounds in disease prevention, disease treatment, and life extension in humans and animals. The invention also relates to methods of preparing ethoxylated polyphenolic compounds, and preparation of compositions comprising the compounds, including dietary supplements and foods. The inventors describe how modified C-glycosidic ellagitannins are safe, palatable and effective at medium and high doses, and produce broad and profound health outcomes in mammals.
US20110092554 1,3,5 tri-subtituted benzenes for treatment of alzheimer's disease and other disorders The present disclosure relates to novel 1,3,5 tri-substituted benzenes of general formula (I), (II) or (III) and the use of such compounds in the treatment of diseases associated with the deposition of -amyloid in the brain.
US20070224204 Combination therapy of respiratory diseases using antibodies and anti-inflammatory agents Therapeutically effective anti-viral compositions, useful especially against respiratory diseases caused or mediated by respiratory syncytial virus (RSV) are disclosed, wherein said compositions comprise at least one anti-RSV antibody, including high affinity antibodies, and an additional anti-inflammatory agent, especially corticosteroids, as well as anti-inflammatory antibodies, especially anti-interleukin-6. Also disclosed are methods of using such compositions to treat and/or prevent respiratory diseases. Such compositions may optionally contain other non-antibody anti-viral agents.
US20110009473 Pttg1 as a biomarker for cancer treatment The present invention relates to the use of pituitary tumor transforming gene 1 (PTTG1) as a biomarker for diagnosing cancer as well as for determining cancer treatment responsiveness. In one embodiment, the present invention provides a method of treating cancer by inhibiting the expression of PTTG1, and administering a therapeutically effective amount of Aurora kinase inhibitor, HDAC inhibitor and/or ROS-generating agent.
CN1582945A Powder injections of composite monoammonium glycyrrhizinate and their preparation A powder injection of compound monoammonium glycyrrhizinate is prepared from monoamononium glycyrrhizinate, glycine, L-cysteine hydrochloride, anhydrous sodium sulfite, sodium chloride solution, sodium hydroxide solution, and aseptic water for injection.
CN103505478A Lucid ganoderma-Cordyceps sinensis granule and preparation method thereof The invention discloses a lucid ganoderma-Cordyceps sinensis granule. A preparation method for the granule comprises the following steps: subjecting purely natural lucid ganoderma to reflux extraction with 70 to 90% ethanol, carrying out pressure reduced condensation, settlement with a ZTC clarifying agent and combination of extracts obtained after extraction three times, filtering the combined extract, then carrying out standing for 10 to 25 h and centrifugation, collecting a precipitate, adding distilled water to dissolve the precipitate, boiling the dissolved precipitate, filtering out insoluble substances while the dissolved precipitate is hot, adding ethanol into an obtained filtrate with stirring until alcohol content reaches 80%, carrying out standing to allow a grayish purple precipitate to be precipitated, drying the grayish purple precipitate at a low temperature to obtain a crude lucid ganoderma polysaccharide product, subjecting the crude lucid ganoderma polysaccharide product to repeated washing and precipitation with 50 to 80% ethanol, carrying out continuous elution and dissolution by using distilled water, concentrating an eluate, adding ethanol until alcohol content reaches 70%, carrying out standing to allow a precipitate to be filtered and drying the precipitate at a low temperature so as to obtain lucid ganoderma polysaccharide; and processing a lucid ganoderma extract particle from 50 to 80% of the lucid ganoderma polysaccharide and mixing the particle and Cordyceps sinensis mycelia according to a ratio of 1: 9 so as to prepare the lucid ganoderma-Cordyceps sinensis granule. The lucid ganoderma-Cordyceps sinensis granule provided by the invention has an immunoloregulation function, enables negative conversion of a hepatitis B surface antigen to be realized and has energy invigorating, foundation strengthening, liver and kidney nourishing, blood circulation promoting and blood stasis removing effects.
US20080058290 Substituted Phenoxy-and Phenylthio-Derivatives for Treating Proliferative Disorders Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
US20100004258 Novel Heterocyclic NF-kB Inhibitors The present invention relates to compounds of the general formula (III): or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof.
CN101756921A Hydroxyurea tablet and preparation method thereof The invention relates to a chemical drug preparation, in particular to a hydroxyurea tablet prepared by taking hydroxyurea as the main ingredient and adding a good amount of adjuvant materials. The raw adjuvant materials include the following ingredients according to the weight proportion: 80-90 percent of hydroxyurea, 5-10 percent of pregelatinized starch, 3-8 percent of super fine silicon dioxide and 0.05-0.5 percent of magnesium stearate. By adopting the technology that powder is directly compressed into tablets, the invention eliminates the pelletization procedure, avoids the problem of hydroxyurea degradation in the pelletization and drying processes and has the advantages of low content of relevant substances and short preparation flow.
US20050080099 Methods and kits for treating depression or preventing deterioration of cognitive function The present invention provides methods and kits for treating depression, perimenopausal depression, schizophrenia, anxiety, panic attacks, binge eating, social phobia, or preventing deterioration of cognitive function by administering to a patient in need thereof a therapeutically effect amount of an estrogen agonist/antagonist of formula I
US20100099677 Compounds, Compositions and Methods Comprising Thiazole Derivatives The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-V) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
US20110306586 NMDA Receptor Modulators and Uses Thereof Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
CN103655504A Dexketoprofen trometamol quick-release/sustained-release double-layer tablet and preparation method thereof The invention relates to a dexketoprofen trometamol quick-release/sustained-release double-layer tablet and a preparation method thereof, and provides a simple and convenient preparation process method for pressing the double-layer tablet consisting of a quick-release layer and a sustained-release layer, wherein the quick-release layer mainly comprises dexketoprofen trometamol, a sustained-release, a diluent, a binding agent and a lubricant. According to the dexketoprofen trometamol quick-release/sustained-release double-layer tablet provided by the invention, due to release of the quick-release part, the medicine is enabled to rapidly achieve effective blood concentration, the sustained-release part can be released slowly, and the effect that the dexketoprofen trometamol can be continuously released for 12 hours when being taken once is achieved. The defects that the conventional dexketoprofen trometamol preparation needs to be taken for multiple times in clinical treatment, and the blood concentration is not stable are made up, so that the effects of improving compliance of patients, stable curative effect and small toxic and side effects are achieved. The tablet is simple in preparation method, raw materials and auxiliaries can be easily obtained, and the tablet is applicable to industrial production and has a good application prospect.
CN103739655A 28-O-beta-D-glucosyl senegenin, and preparation method and application thereof The invention relates to the field of biological medicines, and particularly discloses a 28-O-beta-D-glucosyl senegenin (I) and a preparation method thereof by biotransforming senegenin by a strain with the collection number of NRRL1086. The invention also discloses application of the 28-O-beta-D-glucosyl senegenin in the anti-inflammatory aspect.
US7220757 Topically administering to the patient an antibacterially effective amount compounds such as N-(4,5-Dibromothien-2-ylmethyl)-N'-(1H-imidazo[4,5-b]pyridine-2-yl)-propane-1,3-diamine for therapy of bacterial infection Compounds of formula (I): are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.
US7659387 Transgenic mammals introduced a Period 1 promoter that confers rhythmical expression The present invention relates to an isolated Period 1 (Per1) promoter DNA inducing rhythmical expression of a gene operably linked thereto. This invention also provides a DNA comprising a Period 1 promoter DNA and a gene operably linked thereto, the gene being under the regulation of the promoter DNA. The present invention further provides transformants and transgenic mammals into which the DNA has been introduced. The transformants and transgenic mammals are useful in the screening of pharmaceutical drugs against diseases and disorders pertaining to the circadian rhythm.
CA2815109A1 Cysteine and food intake The present invention relates to the field of nutrition; in particular to the prevention and/or treatment of malnutrition. One embodiment of the present invention relates to a nutritional composition enriched in cysteine for use in the treatment and/or prevention of malnutrition and disorders related thereto. Such a composition may in particular, but not exclusively, be useful for the elderly population.
WO2007025488A1 Method of production of fine-crystalline mixture containing non-steroid anti-inflammatory drug, fine-crystalline mixture obtainable by this method and solid pharmaceutical composition containing this mixture The invention concerns a method of production of a fine-crystalline mixture containing a non-steroid anti-inflammatory drug and an auxiliary substance, wherein a coarse-crystalline substance from the group of non-steroid anti-inflammatory drugs is dissolved in a solvent at an increased temperature, the solution is subsequently distributed at rapid chilling into a cooling liquid containing the auxiliary substance, said cooling liquid being placed in an ice bath, and the product is then filtered off and dried. It further concerns the fine-crystalline mixture of the non-steroid anti-inflammatory drug and the auxiliary substance that can be obtained by the said method. The invention further concerns a solid pharmaceutical composition, having substantially improved dissolution properties, which contains 60 to 78 % w/w of the fine-crystalline mixture, 17 to 40 % w/w of microcrystalline cellulose, colloidal silicon dioxide in an amount of up to 0.3 % w/w, a disintegrant in an amount of up to 4 % w/w and optionally a surface active compound in an amount of up to 0.1 % w/w. This solid pharmaceutical composition can be filled into capsules or used for the preparation of tablets.
US20090220433 Novel biotinylated compositions Novel biotinylated composition comprising a nucleic acid, e.g. siRNA, that are useful for targeting therapeutic and imaging agents to sites of infection and tumors are disclosed.
CN1742738A Pharmaceutical compositions for cancer therapy The medicine composite for curing cancer is composed of dammarane aglycone and its ligand. Its composition is as follows: dammarane aglycone diolsapogenin a PPD is 10%-90%, dammarane aglycone trialspogenin a PPT is 1%-40%, dammarane sapogenin PAM-120 is 1%-20% and PBM-110 is 1%-20%. Said invention also discloses an intravenous injection for curing carcinomatosis. Every 1000ml of said intravenous injection contains 10g of the above-mentioned medicine composite, 130g of cremophor EL, 100ml of absolute ethyl alcohol and the rest is water for injection.
US20110196043 Methods and compositions for administration of trpv1 agonists Compositions are provided that contain a TRPV1 agonist, such as capsaicin, and a solvent system. Topical application of the composition results in rapid delivery of agonist to the dermis and epidermis. Method of using the compositions for reducing nociceptive nerve fiber function in subjects, and for treatment of capsaicin-responsive conditions are also provided.
CN101357918A Penem derivative containing isothioureido sulfhydryl pyrrolidine The invention relates to an ertapenem derivative which contains heter-thioureido sulfhydryl pyrrolidine, the ester which is easy to be hydrolyzed, the salt acceptable in pharmacy, the isomer thereof, the hydrate thereof and the hydrate of ester or salt thereof shown in the formula (I) and a preparing method of the compound shown in the formula (I). The compounds are used as active materials, in particular to be used for preparing the medicine for curing or preventing infectious diseases and to be used as a drug combination containing the compound shown in the formula (I). In the formula (I), the definitions of R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, and n are elaborately described in an introduction.
WO2012105798A3 Composition containing chlorogenic acid for preventing or treating gastroesophageal reflux disease The present invention relates to a pharmaceutical composition for preventing or treating gastroesophageal reflux disease and to a food composition for preventing or treating gastroesophageal flux disease, which contain chlorogenic acid, the pharmaceutically acceptable salts thereof, or derivatives thereof. The present invention also relates to a method for preventing or treating gastroesophageal reflux disease comprising a step of administrating said pharmaceutical composition to an entity, and to the use of chlorogenic acid, the pharmaceutically acceptable salts thereof, or derivatives thereof. According to the present invention, chlorogenic acid, the pharmaceutically acceptable salts thereof, or derivatives thereof may reduce the area of lesions in the esophagus caused by the reflux of the contents of the stomach or duodenum to the esophagus, without changing the pH level in the stomach, and may reduce histological changes of inflammatory cells, and therefore may be valuably used in preventing or treating gastroesophageal reflux disease with no side effects.
CN103622912A Doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation and preparation method thereof The invention adopts the technical scheme that a doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation is provided. According to the technical scheme adopted by the invention, a water-soluble medicine and a fat-soluble medicine are encapsulated by liposome simultaneously; the water-soluble medicine is wrapped with the inner environment of the liposome; the fat-soluble medicine is wrapped between double layers of phospholipid membranes of the liposome; the water-soluble medicine is doxorubicin hydrochloride; and the fat-soluble medicine is docetaxel or paclitaxel. The doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation has the benefits that experiments prove that the toxic or side effect of the doxorubicin hydrochloride-docetaxel or paclitaxel liposome is obviously reduced and the anti-tumor therapy function of the doxorubicin hydrochloride-docetaxel or paclitaxel liposome is enhanced; the medicine encapsulation ratio of the liposome can reach 90% above; the result of the two-year stability experiment of the freeze-dried powder of the liposome at 2 to 8 DEG C below shows that the change rate of the average grain size is less than 6% and the change rate of the medicine encapsulation ratio is less than 5%, and shows excellent stability of the doxorubicin hydrochloride-docetaxel or paclitaxel liposome preparation.
CN101743963B Mosquito repellent and preparation method thereof The invention relates to insect repellents, in particular to a mosquito repellent and a preparation method thereof, wherein the mosquito repellent is characterized by comprising the following components in parts by weight: 1-5 parts of paeonol, 1-5 parts of methyl vanillin, 1-5 parts of ethyl vanillin, 0.5-2.0 parts of vanillin and 80-100 parts of 70% ethanol; and the preparation method of the mosquito repellent is characterized by the following steps: adding the 1-5 parts of paeonol, 1-5 parts of methyl vanillin, 1-5 parts of ethyl vanillin and 0.5-2.0 parts of vanillin into the 80-100 partsof 70% ethanol in parts by weight, mixing, stirring and dissolving to obtain the finished product. The mosquito repellent has wide mosquito repelling scope, long time of prescription, easily obtainable materials and simple process.
US20120207679 Novel Heteroaryl Substituted Benzothiazoles The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.
CN101269030A Domperidone sustained-release dropping pill and preparation method thereof The invention relates to a drug compound having a kinetogenic effect on gastrointestinal and is used for treating dyspepsia, abdominal distension, belch, nausea and vomiting. The drug compound aims to supplement the deficiency of the prior domperidone dropping pill and provide a sustained-release domperidone dropping pill which has fast effect, long-lasting effect, low frequency of drug taking, low cost, high bioavailability and low production cost. The sustained-release domperidone dropping pill adopts domperidone as the ingredient and is prepared jointly with the medicinal carrier used as the stroma.
CN103638036A Application of cardenolide compound in preparation of drugs treating sepsis immunoparalysis The invention relates to application of a compound with a cardenolide structural parent nucleus in treatment of sepsis immunoparalysis. Plant-derived ouabain is employed in the invention, and experiments show that the compound can obviously reverse the simulating clinical sepsis immunoparalysis mice's survival rate caused by cecal ligation and puncture and salmonella secondary hit, and inhibits the decrease of immunoparalysis mice's spleen and lymph node CD4<+> and CD8<+> cells. In clinical severe sepsis patients' blood mononuclear cells, ouabain can reverse sepsis caused mononuclear cell antigen presentation ability reduction and the expression level reduction of TNF-alpha, GM-CSF, IFN-gamma and other TH1 immunostimulation factors. On an LPS (lipopolysaccharide) induced normal human mononuclear intracellular toxin tolerance model, ouabain can effectively reverse mononuclear TNF alpha expressive ability reduction caused by secondary LPS hit. Drugs for effective treatment of sepsis immunoparalysis are lacked clinically at present. Especially under the circumstance of small molecular drugs, the compound has very good development value and application prospects.
US7381710 Nucleic acid comprising a sequence encoding promyelocytic leukemia retinoic acid receptor alpha and a non-immunosuppressive inducer of tumor cell apoptosis which is arsenic; all-trans, 9-cis or 13-cis retinoic acid; or 4 allopurinol-l-ribonucleoside The present invention relates to the combination of a DNA vaccination strategy that makes use of a nucleic acid encoding an immunogenic polypeptide, with a non-immunosuppressive inducer of tumor cell differentiation and/or apoptosis or a tumor cell modifier, useful for cancer therapy. Vaccine compositions and kits are provided, as well as specific nucleic acid constructs that are particularly suitable for the preparation of such compositions.
WO2012020272A3 New salts, polymorphs and solvates of febuxostat The present invention relates to new salts of febuxostat formed by inorganic or organic acids or bases, to a new polymorh and solvate of febuxostat and the invention relates to their production and their use primarily for the prevention or treatment of gout or hyperuricemia.
WO2006132197A1 HETEROCYCLIC COMPOUND HAVING TYPE I 11β HYDROXYSTEROID DEHYDROGENASE INHIBITORY ACTIVITY Disclosed is a compound useful as a type I 11β hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: wherein R1 represents a cycloalkyl which may be substituted, a cycloalkenyl which may be substituted or the like; one of R2 and R3 represents a group represented by the formula: -C(=O)-Y-R4 (where Y represents a group represented by the formula: -NR9- or the like; R4 represents a cycloalkyl which may be substituted or the like; R9 represents a hydrogen or an alkyl which may be substituted; and W represents an alkylene which may be substituted) and the other represents a group represented by the formula: -V-R5 (where V represents a single bond, -O- or the like; R6 represents a hydrogen or an alkyl which may be substituted; and R5 represents a hydrogen, an alkyl which may be substituted or the like); X represents a single bond, -S-, -SO- or the like; U represents a single bond or an alkylene which may be substituted; R7 represents a hydrogen or an alkyl which may be substituted; Z represents -S-, -O- or -NR8-; and R8 represents a hydrogen, an alkyl which may be substituted), a pharmaceutically acceptable salt thereof or a solvate of the compound or salt.
CN1969923A Antivirus extract of isatis root, its extraction method, use and content assaying method The invention discloses an extracting method of antiviral active material based on Cruciferae wade root and leaf as raw material, which is characterized by the following: the extract is adsorbed by large-hole resin, which possesses clemastanin B and active compound with general formula (I); the extract can make antiviral oral or non-oral agent with fitful excipient, which utilizes HPLC method to test content.
US20060241181 Alpha-ketoglutarates of active ingredients and compositions containing same Novel stable and pharmacologically acceptable salts of L-carnitine and lower alkanoyl L-carnitines with alpha-ketoglutaric acid are disclosed as well as the compositions useful as dietary and dietetic supplements, nutraceuticals or drugs containing same.
EP2687507A1 Nitrogen-containing condensed heterocyclic compound There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group, RB represents a C4-18 alkyl group, a C3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II): wherein V represents the formula -CR11R12-, -CO-, -CO-O-, or -CO-NH-, W represents a single bond or a C1-3 alkylene group, and Ring B represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group, Y represents a nitrogen atom or the formula N+(RF), RF represents a C1-4 alkyl group, and m and n, which may be the same or different, each represent an integer of 0 or 1.
WO2008090565B1 Novel thermodynamically stable polymorphic form-l of letrozole The present invention relates to a novel crystalline Form L of letrozole and a process for preparing the same. Letrozole is useful for the first-line treatment in post-menopausal women with hormone receptor positive (or) locally advanced (or) metastatic breast cancer.
WO2008154820A1 Carbethoxy-substituted thiazolyl dihydropyrimidines Novel thiazolyl dihydropyrimidines containing sulfoxide and sulfone, compositions thereof with other antiviral agents, suitable for combating hepatitis B virus (HBV) infections.
CN103212077A Application of Erbin inhibitor in preparation of antitumor drug The invention provides application of an Erbin inhibitor in preparation of an antitumor drug. The inhibitor is specifically a compound capable of lowering expression of Erbin or interfering Erbin-ErbB2 interaction. The Erbin-Erbin interaction is crucial to tumor-prompting action and carcinogenic action of ErbB2; the ErbB2 dependent cancer cell proliferation or tumor growth can be inhibited by over-expressing a PDZ structural segment of Erbin or excessively giving tail-end polypeptide segments to the ErB2 in the cell. The invention provides a novel way of treating ErbB2 positive tumors, i.e., a way of inhibiting protein stability and kinase activity of the ErbB2 by reducing the expression of Erbin or interfering with the combination of ErBin and ErbB2, so that the tumor-prompting action and carcinogenic action of the ErbB2 are inhibited.
CN102850208A Enyne bromide compounds and preparation method and use thereof The present invention relates to enyne bromide compounds (with structural formula shown below) and preparation method and use thereof. Vitro biological activity test shows such compounds significantly inhibit the activity of pancreatic lipase, and can be used as a new drug lead compound for prevention or therapeutic treatment of obesity and related metabolic disorders and used for the preparation of the drug for clinical treatment of common obesity and related metabolic diseases.
WO2007041936A1 Alkyl alcohol piperazine derivative optical isomers and their salts and applications thereof The present application has disclosed preparation methods of aralkyl alcohol piperazine derivative optical isomers of the following general formula (I) and their salts and applications thereof. The activity of antidepression of the present optical isomers are better than present clinical antidepression agents of single inhibiting effect such as desipramine,fluoxetine or antidepression agents of double inhibiting effect such as Venlafaxine, Dutoxetine as they may have wider indications and smaller nerve side effect.
US20100004314 Use of sirna to achieve down regulation of an endogenous gene in combination with the use of a sense construct to achieve expression of a polynucleotide The present invention relates to the combinatorial use of an siRNA targeted against an endogenous gene to knock out or knock down expression of the endogenous gene in a host and a delivery of a polynucleotide encoding the gene in a delivery vehicle/expression vector to the host to provide expression in the host of the protein encoded by the polynucleotide.
US20110158920 Method of producing a composition from an oleogel and an aqueous gel and the composition A method for producing a bigel, the method comprising: (a) providing an oleogel comprising at least one oily agent gelled with at least one cellulose polymer; (b) providing an aqueous gel comprising at least one component whose viscosity is pH dependent, such as a carbomer; (c) mixing the oleogel and the aqueous gel together to form a bigel; and (d) subsequently adjusting the viscosity of the bigel under high flow and low shear stirring to obtain a bigel of a desired viscosity.
CN101229190A Method for preparing highly water-soluble cydiodine The invention discloses a preparation method of a high water-soluble cydiodine, which belongs to pharmacy technology field. Quickly putting the iodine solution into Beta- cyclodextrin saturated solution and then mixing constantly until the solution cools to below 40 DEG C. Then naturally precipitating the cooled cydiodine solution and pouring the supernatant out and leaving the sediment when the precipitation completes. Or separating the cooled cydiodine solution via centrifugation to separate the sediment and water, and then putting the sediment to the oven to bake to powder and then sift out; in addition, spray drying the cooled west ground solution to get dry powder of cydiodine is also feasible. Put the dry cydiodine powder to the oven to bake for a certain period and then mixing well, and the high water-soluble cydiodine will be formed. The high water-soluble cydiodine prepared by the method has the advantages of having fast coating speed, high water-soluble, good disinfect effect and stable quality.
CN1593443A Medical phytoestrogen Disclosed is a medical phytoestrogen which is characterized by that, the content of total flavones of root of kudzu vine is at least 1mg/kg weight of human body. It is safe and effective to be the substitute of the chemical phytoestrogen. The medical phytoestrogen can be used as medicine or as health product.
US20060178295 androgen steroid conjugated with one or more mammalian proteins; diagnosis or treatment of solid cancer and hematological malignancies; exhibit a synergistic action together with a cytoskeleton-acting drug such as Taxol (reg); prostate cancer Conjugates comprising one or more steroids conjugated with one or more mammalian proteins are disclosed. The conjugates are useful for diagnosis or treatment of solid cancer and hematological malignancies. Further the conjugates exhibit a synergistic action together with a cytoskeleton-acting drug such as Taxol®, which enable the treatment of cancers that otherwise would be non-responsive to Taxol®.
EP2748162A1 2 -amino-4 - (pyridin- 2 -yl) - 5, 6 -dihydro-4h- 1, 3 -oxazine derivatives and their use as bace-1 and/or bace - 2 inhibitors The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
CN102186473A Compounds for the treatment of peripheral neuropathies A compound of formula A1 or A2 for use in the treatment of a demyelinating peripheral neuropathy: wherein A is COOR5, OPO(OR5)2, PO(OR5)2, SO2OR5, POR5OR5 or 1H-tetrazol-5-yl, R5 being H or an ester-forming group, optionally C1-6alkyl; W is a bond, C1-3alkylene or C2-3alkenylene; Y is C6-10aryl or C2-9heteroaryl eg C3-9heteroaryl, optionally substituted by 1 to 3 radicals selected from halogen, OH, NO2, C1-6alkyl, C1-6alkoxy; halo-substituted C1-6alkyl and halo-substituted C1-6alkoxy; Z is chosen from Formula (I) : wherein the asterisks of Z indicate the point of attachment between -C(R3)(R4)- and A of Formula (Ia) or (Ib), respectively; R6 is chosen from hydrogen and C1-6alkyl; and J1 and J2 are independently methylene or a heteroatom chosen from S, O and NR5; wherein R5 is chosen from hydrogen and C1-6alkyl; and any alkylene of Z can be further substituted by one to three radicals chosen from halo, hydroxy, C1-6alkyl; or R6 can be attached to a carbon atom of Y to form a 5-7 member ring; R1 is C6-10aryl or C2-9heteroaryl eg C3-9heteroaryl, optionally substituted by C1-6alkyl, C6-10aryl, C6-10arylC1-4alkyl, C3-9heteroaryl, C3-9heteroarylC1-4alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl, C3-8heterocycloalkyl or C3-8heterocycloalkylC1-4alkyl; wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl of R1 may be substituted by 1 to 5 groups selected from halogen, C1-6alkyl, C1-6alkoxy and halo substituted-C1-6alkyl or -C1-6alkoxy; R2 is H, C1-6alkyl, halo substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; and each of R3 and R4, independently, is H, halogen, OH, C1-6alkyl, C1-6alkoxy or halo substituted C1-6alkyl or C1-6alkoxy; and the N-oxide derivatives thereof or prodrugs thereof, or a pharmacologically acceptable salt, solvate or hydrate thereof.
EP2260863A1 Prophylactic/therapeutic agent for infectious disease Disclosed is a prophylactic or therapeutic agent for bacterial infectious diseases, which comprises an antibody capable of binding to a toxin or an antitoxin that constitutes a bacterial toxin-antitoxin system to inhibit the interaction between the toxin and the antitoxin or a gene for the antibody as an active ingredient.
US20130045204 Fluorinated bisphenol ether compounds and methods for their use Compounds having a structure of Formula I: or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein, and wherein at least one of R1, R2, R3, R4 or R5 is F, are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.
WO2011113309A1 Pyrimidine derivatives for use as sphingosine 1-phosphate 1 (s1p1) receptor agonists Disclosed are pyrimidine derivatives for use as sphingosine 1- phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or diseases mediated by S1P1 receptors, particularly multiple sclerosis.
US20100215736 Oral dosage form providing fast adsorption of drug The invention relates to a certain oral dosage form providing absorption of the drug diclofenac in an ultrafast manner.
CN103127099A Amoxicillin potassium clavulanate dry suspension and production process thereof The invention discloses amoxicillin potassium clavulanate dry suspension and a production process thereof. The amoxicillin potassium clavulanate dry suspension is prepared from amoxicillin, potassium clavulanate, hydroxy propyl methylcellulose and the like in a mixing manner. The amoxicillin potassium clavulanate dry suspension has good compliance to a user.
US20070275978 Of at Use of an Antagonist Compound of at Least One Receptor Selected From a Group Comprising Beta-Adrenergic Receptors, A at1, 5-Ht5 and Galanin Receptor for Preparing a Pharmaceutical Composition for Treating Rosacea The invention relates to the use of an antagonist of at least one receptor chosen from the group comprising the beta-adrenergic receptors, the AT1 receptor, the 5-HT2 receptor, the 5-HT5 receptor and the galanin receptor, for the preparation of a pharmaceutical composition for treating rosacea.
US20060134286 Gallocatechin gallate-containing composition The present invention provides a safe and highly effective antibacterial composition without impairing the flavor of foods or drinks, which composition is used in products such as foods and oral care goods which are mainly to be taken into human or animal bodies or mainly to be used in the oral cavity. The composition according to the present invention contains gallocatechin gallate as an agent for enhancing the activity of antibacterial catechins in which the antibacterial activity of the antibacterial catechins against Streptococcus mutans is particularly enhanced. The composition according to the present invention can be produced by mixing the antibacterial catechins with gallocatechin gallate. Alternatively, it can be produced as a composition comprising a synthetic adsorbent-adsorbed fraction as the main component, which is obtained by subjecting a solvent-extract from tea leaves to an adsorption treatment with the use of a synthetic adsorbent selected from among aromatic compound-based synthetic adsorbents and methacrylic compound-based synthetic adsorbents.
CN101357140A Vitamin-adding high-peptide pearl active calcium replenishing agent and preparation method thereof The invention relates to a Garvey high-peptide and pearl-activity calcium supplement and a preparation method thereof, belonging to the technical field of food processing; the calcium supplement comprises 5 to 80 percent of water-soluble mixed pearl calcium powder, 5 to 50 percent of high-peptide powder of clam meat, 1 to10 percent of vitamin and corresponding conventional auxiliary materials, and the preparation method is characterized in that both the water-soluble mixed active pearl calcium powder and the high-peptide powder of clam meat are made by treating the pearls and the clam meat with the pearls removed by grinding, enzyme degradation, acid degradation, filtration and other processes; and the calcium, magnesium and other elements contained exist in the inorganic state and the organic state and the content of protein peptide is increased, so as to meet the needs of human body for inorganic calcium, organic calcium and special protein peptide and to be conducive to human health and longevity. In addition, a plurality of vitamins are contained, therefore, the active calcium supplement has the advantages of rich nutrition, and easy absorption, transformation and utilization for the human body, etc. The Garvey high-peptide and pearl-activity calcium supplement can be added with different auxiliary materials, and can be made into capsules, tablets, effervescent tablets and other dosage forms by the conventional mechanical preparation method, so as to facilitate promotion and application.
WO2006066950A2 Tricyclic aminoalcohols, methods for producing the same and their use as anti-inflammatory agents The invention relates to the tricyclic aminoalcohols of general formula (I), to methods for producing the same and to their use as anti-inflammatory agents.
US7507746 Enantiomer of tenatoprazole and the use thereof in therapy This invention relates to optically active substances of tenatoprazole, (+) and (−)-5-methoxy-2-{(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}-1H-imidazo[4,5-b]pyridine. The compound and pharmaceutical compositions thereof are useful for anti-ulcer agent.
WO2013140347A1 Sulphonamide derivatives of benzylamine for the treatment of cns diseases Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted;or 9-or 10-membered bicyclic group, linked to –(O) x - (CH 2 ) y -through one of its aromatic carbon atoms,consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5-or 6-membered non-aromaticheterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1 -C3 - alkyls; D represents a group selected from:phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted;thiophene unsubstituted or substituted;bicyclic group consisting of imidazolering fused with5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2heteroatoms independently selected from the group consisting of N, O and S, unsubstituted or substituted and linked to sulphonamide moiety through one of carbon atoms of benzene ring;and bicyclic group consisting of benzene ring fused with -or 6-membered non-aromatic heterocyclic ring having 1 or 2heteroatoms independently selected from the group consisting of N and O, unsubstituted or substituted, and linked to sulphonamide moiety through one of carbon atoms of benzene ring;R represents H or –CH 3;x is 0 or 1;yis 2 or 3;and pharmaceutically acceptable salts and solvates thereof, with the provisos that if x is 0 and y is 2, then D is naphthyl unsubstituted or substituted with one halogen atom, and if R represents –CH 3, then A is not unsubstituted or substituted phenyl. The compounds can be used in the treatment and/or prophylaxis of central nervous system disorders.
US20110201575 Stabilized solid dispersion of adefovir dipivoxil and preparation method thereof The present invention relates to an amorphous solid dispersion with improved stability comprising 9-[2-[[bis[(pivaloyloxy)methyl]phosphono]methoxy]ethyl]adenine as a nucleotide analogue, a pharmaceutical composition comprising the same, and a method for preparing the same.
EP2019099A1 Dpp-IV inhibitors The invention relates to compounds of formula (I) wherein R1, R2, R3 and n have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.
CN102249978A KY crystal form of Atorvastatin calcium and preparation method thereof The invention relates to a new crystal form of Atorvastatin calcium, namely KY crystal form. Expressed in interplanar distance (d), the characteristic peak of the crystal under X-ray powder diffraction conditions is 3.03; or the crystal is (2theta) 5.389 degrees, 8.799 degrees, 11.573 degrees, 18.892 degrees and 28.116 degrees under X-ray powder diffraction conditions. In the differential thermal analysis map (DSC map) of the crystal, characteristic endothermic peaks are arranged at about 44.0 DEG C, 148.6 DEG C, 166.8 DEG C and 252.9 DEG C. The invention also relates to a method for preparing the crystal form and a medical composition containing the crystal form.
CN1739510A Use of sophoridine oxide in preparing anticancer medicine The present invention relates to the use of sophoridine oxide in preparing medicine for treating adenocarcinomas, including breast carcinoma, lung carcinoma, intestinal cancer and other cancer on gland. Sophoridine oxide in effective treating amount and pharmaceutically acceptable supplementary material are used in preparing the medicine in the forms one freeze dried powder for injection, soft capsule, dripping pill, coated tablet, etc. Sophoridine oxide has anticancer activity higher than that of sophoridine and toxic side effect less than that of sophoridine.
CN102552282A Transdermal absorption medicament used for skins and comprising adjuvant-containing methylprednisolone aceponate and adjuvant-containing water The invention relates to a transdermal absorption medicament used for skins and comprising adjuvant-containing methylprednisolone aceponate and adjuvant-containing water. The medicament comprises individually packaged methylprednisolone aceponate which contains one or several solid pharmaceutic adjuvants, is insoluble in water and has D90 particle sizes of 0.1-10mum, and individually packaged water containing one or several pharmaceutic adjuvants soluble in water.
CN103550226A Compound sulfamonomethoxine sodium injection as well as preparation method thereof The invention discloses a compound sulfamonomethoxine sodium injection, and relates to the field of preparation of veterinary medicines. The compound sulfamonomethoxine sodium injection is prepared from medicines and auxiliary materials such as sulfamonomethoxine sodium, propylene glycol, ethanol, an antioxidant, EDTA (Ethylene Diamine Tetraacetic Acid) and potassium clavulanate. The invention further provides a preparation method of the compound sulfamonomethoxine sodium injection. The compound sulfamonomethoxine sodium injection disclosed by the invention as a novel veterinary compound preparation can be effective by one injection for frequently occurred epidemic mixed influenza. The compound sulfamonomethoxine sodium injection disclosed by the invention has a unique curative effect to porcine contagious pleuropneumonia, cough and enzootic pneumoniae. The compound sulfamonomethoxine sodium injection is superior to a common medicine florfenicol in both curative effect and porcine weight increment.
WO2013067141A1 N- (3- { [ (3- { [2-chloro-5- (methoxy) phenyl] amino} quinoxalin- 2 -yl) amino] sulfonyl} phe nyl) - 2 -methylalaninamide as phosphatidylinositol 3 - kinase inhibitor for the treatment of lymphoproliferative malignancies Methods are provided for treating a lymphoproliferative malignancy to a patient in need of such treatment, comprising administering to the patient an effective amount of compoud A as described herein.
CA2816554A1 Use of 2',5'-oligoadenylate derivative compounds The invention relates to the therapeutic uses of 2',5'-oligoadenylate derivative compounds, more particularly for the treatment of chronic fatigue syndrome (CFS) and in the treatment of infection by a gamma-retrovirus.
US7488733 For improving perception, concentration, learning or memory; 2-(Cyclopentylmethyl)-4-[(fluorophenyl)amino]6-oxo-1,6-dihydro-5-pyrimidinecarbonitrile; amination of methyl 2-cyano propenoate derivatives, cyclization using amidinehydrochloride derivatives The invention relates to novel 6-arylamino-5-cyano-4-pyrimidinones of formula (I) methods for the production thereof, and the use thereof for producing medicaments utilized for improving awareness, concentration, learning capacity, and/or retentiveness of memory. Said compounds (I) show activity as PDE9 inhibitors.
WO2012009973A1 Antiparkinsonian drug-loaded microsphere composition and use thereof An antiparkinsonian drug-loaded microsphere composition and the use thereof for preparing the medicine for the precaution or treatment of Parkinson's disease or its complications are disclosed. The composition consists of biodegradable hydrophobic polymer and the antiparkinsonian drug. The antiparkinsonian drug is selected from benserazide, melevodopa or their mixtures. The biodegradable hydrophobic polymer is selected from poly(lactic acid), poly(lactic acid-glycolic acid), polycaprolactone or their mixtures.
CN102697723A Methylcantharidinimde fat emulsion and preparation method thereof The invention provides a methylcantharidinimde fat emulsion. A formula of the methylcantharidinimde fat emulsion comprises methylcantharidinimde, fatty oil, a surfactant and an isosmotic regulating agent. According to the methylcantharidinimde fat emulsion, the defect of low solubility of methylcantharidinimde is overcome, a targeting function is realized simultaneously, tissue distribution in the kidney can be reduced, tissue distribution in the liver is increased, the treatment effect is enhanced, and the toxic and side effects are reduced.
WO2007120596A1 DIHYDRO[1,4]DIOXINO[2,3-e]INDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
CN101249087A Applications of isobavachin for preparing antineoplastic, osteoporosis and senile dementia medicament The invention relates to the use of isobavachin in preparing drugs against tumors, osteoporosis and senile dementia, which belongs to the medical field. Isobavachin has the structural formula shown as the figure (I) and a chemical name thereof : 2,3-dihydro-7-hydroxy-2-(4-hydroxyphenyl)-8-(3-methyl-butyl-2-alkenyl)-4H-1-benzopyran-4-one. The compound, in low concentration, doesn't change the expressions of ERalpha66, ERalpha46 and ERalpha36, but in high concentration, inhibits the expressions thereof at the same time. Furthermore, the compound (I) can kill breast cancer cell line MCF7 that expresses ERalpha66, ERalpha46 and ERalpha36. The compound (I) can also be used as regulator of estrogen receptor ERalpha36 to treat diseases caused by abnormal expression of estrogen receptor ERalpha36, such as tumors, osteoporosis, asthma, heart diseases and senile dementia.
WO2006058940A1 Use of amygdalin analogues for the treatment of psoriasis The invention relates to compounds having formula (I), in which n is an integer between 0 and 4; R1 is a radical that is selected from the group containing H, CH3, CH2-CH3, C(CH3)3, COOH, CONH2 and C≡CH; R2, R3, R4 and R5 are radicals that are selected independently from the group containing H, F, Cl, Br, (C1-C3)-alkoxyl and (C1-C4)-alkyl; and R6 is a radical that is selected from the group containing H, F, Cl, Br, (C1-C3)-alkoxyl, (C1-C4)-alkyl, R7, CH=CH-R7 and O-CH2-R7, wherein R7 is phenyl or a phenyl that is mono- or di-substituted independently by F, Cl, Br, (C1-C3)-alkoxyl or (C1-C4)-alkyl. The aforementioned compounds have a chemotactic index similar to amygdalin (a natural product with a chemotactic profile similar to peptide T) and, consequently, can be used for the treatment of allergic and/or inflammatory dermopathies, such as psoriasis, said compounds offering the advantage of being much less toxic than amygdalin.
CN102512524A Medicine for treating secretory otitis media and acute suppurative otitis media A medicine for treating secretory otitis media and acute suppurative otitis media is prepared by uniformly blending borneol, mint, Rhizoma Coptidis, indigo naturalis, alum, gallnut, forsythia, aired fresh pig gallbladder and gardenia in a form of power and in a volume ratio of 2: 1: 1: 0.5: 2: 0.5: 0.5: 2: 0.5.
WO2008092103A9 Combination cancer treatments comprising elsamitrucin and other agents Disclosed herein are methods relating to combination cancer treatments that include elsamitrucin and other agents.
CN1781482A Nizatidine freeze-dried powder injection and preparing method The present invention is freeze-dried Nizatidine powder for injection and its preparation process. The freeze-dried Nizatidine powder for injection has the main components including Nizatidine in 0.25-3 weight portions, water soluble freeze drying supporting agent in 0.1-10 weight portions and co-solvent in 0.1-10 weight portions. The water solution with Nizatidine content of 25 mg/ml has pH value of 5-11.
WO2011154677A1 Substituted n-[1-cyano-2-(phenyl)ethyl] 1-aminocycloalk-1-ylcarboxamide compounds - 760 The present invention provides compounds of formula (I) in which, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
US20070104781 Hypocholesteremic preparations containing mixtures of phytostenol(ester)s and conjugated fatty acids, and methods of using the same A hypocholesteremic preparation containing at least one component (a) selected from the group consisting of phytostenols and phytostenol esters and at least one component (b) selected from conjugated fatty acids having from about 6 to about 24 carbon atoms and glycerides of conjugated fatty acids having from about 6 to about 24 carbon atoms is disclosed. Methods of reducing serum cholesterol content in a mammal via administration of hypocholesteremic preparations described herein are also disclosed.
US6921771 Administering a fused aminoquinoline derivative such as (5R)-5-(methylamino)-5,6-dihydro-4H-imidazo(4,5,1-ij) quinoline-2(1H)-thione or pharmaceutically acceptable salts The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually mating amount is from about 0.003 thru 0.2 mg/kg/dose.
EP2238114A1 Novel imidazolinylmethyl aryl sulfonamides This invention relates to an alpha- 1 A receptor partial agonist, which is represented by Formula (I) and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing formula I, methods for their use as therapeutic agents, and methods of preparation thereof.
CA2835321A1 Compounds for use in the treatment of feline retroviral infections The present invention relates tocompounds and compositions for use in the treatment or prevention of retroviral infections in felines,in particular cats,and to the use of said derivatives for the manufacture of a medicament for the treatment or prevention of feline leukemia virus (FeLV) infections occurring alone or together with feline immunodeficiency virus (FIV) infections in cats.
CN101735335A Water soluble cantharidin and/or norcantharidin chitosan derivative and preparation method thereof The invention belongs to the technical field of medicines and discloses a water soluble cantharidin and/or norcantharidin chitosan derivative and a preparation method thereof. The derivative is obtained after reaction between the chitosan and the cantharidin or norcantharidin (norcantharidin acid and salt thereof). The chitosan derivative is shown as follows, wherein R and R' is respectively and independently selected from the cantharidin or norcantharidin (norcantharidin acid and salt thereof) and n is 0.5-3000 (the molecular weight of the chitosan is 179-1000000). The derivative has good water solubility and low toxic and side effects, and the reaction product has anti-tumor activity, alleviates the vascular stimulation of cantharidin, increases leukocyte and can be used for treating tumors.
CN101953857A Compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder) composite medicine The invention discloses weight ratio of material components of a compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder ) A composite medicine and, weight ratio of material components of a compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder ) B composite medicine, weight ratio of material components of a compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder ) C composite medicine, a preparation method and steps of the compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder ) A composite medicine, a preparation method and steps of the compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder ) B composite medicine, a preparation method and steps of the compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder ) C composite medicine, as well as the application of the compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder ) A composite medicine, the compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder ) B composite medicine and the compound fermented cordyceps sinensis bacterium powder (paecilomyces hepiali Cs-4 bacterium powder ) C composite medicine for anti-aging, antifatigue, anti-hypoxia, immunity enhanced, sedative, antishock and anti irradiation.
US20120225093 Abrogating HIV-1 Infection via Drug-Induced Reactivation of Apoptosis The present invention relates to compositions and methods of treating, inhibiting, or controlling HIV infection.
US7501525 Derivatives of benzimidazole and their use as medicaments A subject of the present Application is novel derivatives of benzimidazole and imidazo-pyridine which have a good affinity for certain sub-types of melanocortin receptors, in particular the MC4 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more melanocortin receptors are involved. The invention also relates to pharmaceutical compositions containing said products.
EP1585740A2 Process to prepare psorospermin Psorospermin and analogs thereof are made using an enantiomerically selective process.
CN103005685A Evening primrose odor type snuff The invention belongs to the technical field of snuff goods, relates to an evening primrose odor type snuff made of pure natural materials, and further relates to a preparation method of the snuff. The snuff consists of the following natural materials according to parts by weight: 100-500 parts of green tea leaf, 0.05-0.35 parts of muskiness, 50-150 parts of flower bud of lily magnolia, 10-90 parts of safflower, 100-300 parts of Herba Artemisiae Capillaris, 0.1-0.4 parts of borneol, 0.03-0.10 parts of asarum, 0.01-0.09 parts of rhinoceros horn, 5-15 parts of rhizoma cyperi, 25-125 parts of tobacco leaf, 2-6 parts of tambac, 2-6 parts of flos caryophylli, 5-25 parts of angelica dahurica, 2-6 parts of menthol crystal and 50-150 parts of red wine. Through evening primrose fumigating, the snuff disclosed by the invention has a delicate fragrance of evening primrose. The snuff disclosed by the invention can produce refreshing effect to the mind, enables a nasal cavity to be ventilated, and can assist to quit smoking.
WO2009028649A1 Method for reduction in volume of solid preparation having high amino acid content Disclosed are: a method for further reducing the volume of an amino acid preparation whose amount of intake per unit time has been increasing; and a preparation. Specifically disclosed are: a method for producing a solid preparation comprising an amino acid as an active ingredient, which comprises the steps of charging a powder comprising the amino acid and a binder into a vessel and kneading and granulating the mixture in one step in the vessel; and a solid preparation having a high amino acid content, which is produced by the method.
US20120108625 Novel forms of tiotropium bromide and processes for preparation thereof This invention relates to novel crystalline forms of tiotropium bromide, processes for preparing them, and their use in pharmaceutical formulations.
CN102112131A Methods of treating thalassemia Provided herein are method of treating, ameliorating, or delaying at least one symptom of a genetic blood disorder, e.g. sickle cell disorder or thalassemia, in a patient in need thereof, comprising administering a therapeutically effective amount of a Jak2 inhibitor. Also provided in part is a method of reducing an enlarged spleen in a patient suffering from thalassemia, comprising administering a therapeutically effective amount of a Jak2 inhibitor.
CN103145676A 7,4'-disubstituted isoflavone derivative and preparation method and application thereof The invention relates to a 7,4'-disubstituted isoflavone derivative and a preparation method and application thereof. The structural formula is shown in the specification, wherein R is 2-hydroxyl-3-di-n-propylaminly propyl, 2-hydroxyl-3-piperidyl propyl, 3-dimethylamino propyl or 3-diethylin propyl. The preparation method of the compound is simple and high in yield. The compound prepared according to the invention has good antitumor activity in vitro.
US20120107406 Dry Powder Formulations A dry powder suitable for inhalation n a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period of time that is less than 60 minutes.
EP2613766A2 Compositions comprising a fatty acid oil mixture comprising epa and dha in free acid form, a surfactant, and a statin Preconcentrates comprising a fatty acid oil mixture, at least one surfactant, and at least one statin or pharmaceutically acceptable salt, hydrate, solvate, or complex thereof, and methods and uses thereof are disclosed. The preconcentrates are capable of forming a self-nanoemulsifying drug delivery system (SNEDDS), a self-microemulsifying drug delivery system (SMEDDS), or self-emulsifying drug delivery systems (SEDDS) in an aqueous solution.
CN1739557A Dietotherapeutic product for preventing and treating primary urate calculi, gout and acalcerosis and its prepn process The dietotherapeutic product for preventing and treating primary urate calculi, gout and acalcerosis consists of salt of organic acid, salt of inorganic acid, nucleotide, vitamin and trace elements. The dietotherapeutic product operates on that the product creates conditions for dissolving urate in water soluble alkali salt and removing and for dissolving calcium salt in acid solution for being absorbed and utilized, the nucleotide avoids purine to synthesize urate, and the vitamin and the trace elements reinforce the activity of enzyme, protect the functions of cell and organ, recover nucleotide and make purine to synthesize essential nucleic acid to reduce purine and urate and avoid urate calculi and gout. The dietotherapeutic product has obvious curative effect, no toxic side effect, simple preparation process, and low cost.
WO2006105194A2 Penciclovir or famciclovir for the treatment of recurrent genital herpes with a one-day application A method for the treatment of recurrent genital herpes, in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a treatment period of one day.
WO2014141287A1 The art, method, manner, process and system of multifunctional nanobiomaterial for molecular imaging and drug- delivery The present invention relates to a nano-sized material that can provide contrast enhancement for multiple molecular imaging mthods and also deliver therapeutic nucleic acids or chemodrugs at a specific site of disease such as cancer. In particular, the present invention relates to a nanosized synthetic calcium apatite based materials showing contrast imaging for visible to near-infrared fluroscence, magnetic resonance imaging and x-ray imaging together with targeted delivery of nucleic acid drugs (DNA or RNA) to specific cancer types.
CN101269017A Rosiglitazone sustained-release dropping pills and preparation method thereof The invention discloses a medicine composition used for curing diabetes mellitus, more particularly relates to a medicine composition oral preparation prepared by taking rosiglitazone or salt thereof as raw material. The invention aims at making up the deficiency of the existing oral pharmaceutical preparation used for curing type II diabetes mellitus, and provides a medicine composition oral preparation rosiglitazone sustained-release pill that has the advantages of high bioavailability, rapid effect, controllable medicine release, long effectual time, few times needed by the patient to take the medicine, low price and no pollution in the production. The rosiglitazone sustained-release pill related by the invention takes the salt of the rosiglitazone as medicine active ingredient and can be prepared together with medicated carrier that takes hydrophilic framework material and hydrophobic framework material as stroma.
CN101804073A Preparation method of pearl producing immune reinforcing agent The invention relates to a preparation method of a pearl producing immune reinforcing agent, which prepares a novel nacre cell flakelet preservative solution-an immune reinforcing agent by taking synthesized a Zn2 plus metal chelate compound as a main material, adding a proper amount of biological tissue fluid as a regulator and finally adding other auxiliary materials. The action mechanism of the method is mainly reducing the molecular recognition ability of the nacre, reducing exclusive reaction and increasing the core retaining rate of the nacre via chemical and biological regulation and control, thereby increasing the yield and quality of pearls and further driving the development of the Nanhai pearl industry so as to prosper the seawater pearl industry in China.
US20110236397 Limited proteolysis of cd2ap and progression of renal disease Compositions which specifically block cathepsin L function in podocytes, compositions which protect cytoskeletal adaptor protein (CD2AP) for degradation, compositions which modulate expression or function of cytoskeletal adaptor protein (CD2AP), protect against renal diseases or disorders. Methods of treatment in vivo involve use of one or more compositions.
US7511026 Therapeutic agent for nerve damage The present invention provides a therapeutic agent for nerve damages such as those caused by spinal cord injury or nerve trauma, which includes, as an active ingredient, a low-molecular-weight saccharide composed of at least glucuronic acid and/or N-acetylglucosamine or a pharmaceutically acceptable salt thereof. The present invention also provides a therapeutic agent for nerve damages which includes, as an active ingredient, preferably a low-molecular-weight hyaluronic acid, more preferably hyaluronic acid disaccharide to hyaluronic acid 2,500-saccharide, further more preferably hyaluronic acid disaccharide to hyaluronic acid 50-saccharide, much more preferably hyaluronic acid tetrasaccharide, or a pharmaceutically acceptable salt thereof.
US20080114024 such as 5-(3-Aminopropylamino)-2-benzyloxy-7-(4-methoxyphenyl)-[1,6]naphthyridine; spleen tyrosine kinase inhibitor; controlling activation of mast cells; antiallergens, antiinflamamtory agents; asthma, chronic obstructive pulmonary disease (COPD), Crohn's disease, bronchitis, conjunctivitis, psoriasis Disclosed are compounds of formula (I): wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
EP1572185A1 Lipoxygenase inhibitors as hypolipidemic and anti-hypertensive agents The present invention provides a method for treating elevated serum triglycerides or hypertension via administering to a human subject with elevated serum triglycerides or hypertension an effective amount of pharmaceutical composition comprising a 5-lipoxygenase inhibitor, in an effective amount which is sufficient to reduce elevated serum triglycerides or hypertension, wherein the 5-lipoxygenase inhibitor is not NDGA or curcumin.
US20120165410 Production of encapsulated nanoparticles at high volume fractions The present invention relates to methods for producing particles of a biologically active material using dry milling processes as well as compositions comprising such materials, medicaments produced using said biologically active materials in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of said biologically active materials administered by way of said medicaments.
WO2007044976A3 Improved testosterone gel and method of use The present invention relates to an improved transdermal hydroalcoholic testosterone gel formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.
US20060270632 4-(2-Furoyl) aminopiperidine compound useful as therapeutic agent for itching There are provided compounds represented by the following general formula (I): [where R1 is 5-methylpyridin-2-yl, p-tolyl or mesityl, R2 is one of the following general formulas (II)-(IX): (where R3 is C1-C4 alkyl, R4 is H or C1-C4 alkyl, R5 is H, 3-pyridylmethyl or 4-pyridylmethyl, and R6 is 2,4-dihydroxybenzyl, 3-pyridylmethyl or 4-pyridylmethyl), or when R1 is mesityl, R2 is the following formula (X)], and pharmaceutically acceptable salts thereof. The compounds exhibit pruritus-inhibiting action, and are useful for prevention or treatment of itching and pruritus caused by reaction against insect-inflicted wounds, reaction against environmental allergens, skin infections or external parasite infections, or caused to renal dialysis patient.
EP2643310A1 4- (5-cyano-pyrazol-1-yl) -piperidine derivatives as gpr 119 modulators Compounds that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein- coupled receptor GPR119 in animals are described herein.
WO2014153356A1 An in vivo intracellular reprogramming composition and method of making and using same A composition comprising a pharmaceutical, a neutraceutical and an optional carbonaceous material wherein the pharmaceutical comprises a biguanide or a substituted biguanide.
US6933321 For therapy of androgen-dependent diseases such as prostate cancer, benign prostatic hyperplasia, precicious puberty, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and premature male baldness Biphenyl derivatives are disclosed for use in the treatment of androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, precocious puberty, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and premature male baldness. For example, some preferred compounds having the structure: are formulated together with pharmaceutically acceptable diluent or carrier for topical use in the treatment of acne, hirutism, seborrhea or androgenic alopecia, or for systemic use in the treatment of androgen-dependent prostate cancer.
US7618988 Use of substituted aminomethyl chromans Compounds of formula I in which R has a meaning as indicated in claim 1, or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders and/or for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics.
US7718649 Physical states of a pharmaceutical drug substance An amorphous form of imipramine pamoate, morphologically pure forms, and mixtures of amorphous and morphologically pure imipramine pamoate characterized by differential scanning calorimetry, fourier transform infrared, and powder x-ray diffraction, and pharmaceutical compositions formed therefrom.
EP1735055A1 Method of reducing c-reactive protein using growth hormone secretagogues The present invention relates to a method of reducing C-reactive protein in a subject in need of treatment thereof, wherein the subject is at risk of having or the subject has already had a vascular event or suffering from an inflammatory disease or disorder. In one embodiment, the vascular event is a cardiovascular event (e.g., myocardial infarction). In another embodiment, the vascular event is a cerebrovascular event (e.g., stroke (such as transient ischemic attacks (TIAs)). In yet another embodiment the vascular event is a peripheral vascular event (e.g., intermittent claudication). The method comprises administering a therapeutically effective amount of at least one growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof. The growth hormone secretagogue can be coadministered with a second growth hormone secretagogue, HMG CoA reductase inhibitor, an ACAT inhibitor, a CETP inhibitor, an anti-inflammatory agent, an ACE inhibitor, a Beta blocker, a cholesterol absorption inhibitor, a nicotonic acid, a fabric acid derivative, a bile acid sequestering agent or a combination thereof.
US7553847 Treating obsessive-compulsive disorder, acute stress disorder, post traumatic stress disorder, social anxiety disorder, somatization disorder; 2-(7-chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-2-oxo-hexyl)-1-isoindolinone The present invention provides methods for treating social anxiety disorder, comprising administering 2-(7-chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-2-oxo-hexyl)-1-isoindolinone or 2-(7-chloro-1,8-naphthyridine-2-yl)-3-(5-methyl-5-hydroxy-2-oxohexyl) -1-isoindolinone or pharmaceutically acceptable salt, or optical isomer therof, and optionally comprising administering another compound for the treatment of social anxiety disorder that is a GABA agonist.
CN102174123B Production method of water soluble flavone-chitosan derivative The invention discloses a production method of a water soluble flavone-chitosan derivative, relating to a preparation method of a flavonoid uvioresistant active substance. The production method takes chitosan and a flavone compound as raw materials, and the product is prepared by the processes of preparing a small molecular chitosan solution, synthesizing a water soluble flavone-chitosan derivative, concentrating and the like. The invention has the advantages of simple method, simplicity of operation, simple equipment, mild reaction conditions, energy conservation, full utilization of material resources in the production process, no discharge of three wastes, benefit to environmental protection, low production cost and convenience of popularization and application; and the product is characterized by being freely soluble in water, having good moistening effect and the like. The product prepared by the invention can be extensively used in skin care cosmetics and medicaments for treating skin diseases.
US20110130428 Sublingual Compositions Comprising (2S) - (4E) -N-Methyl-5- (3- (5-Isopropoxypyridin) YL)-4-Penten-2-Amine The present invention relates to sublingual compositions comprising (2S)-(4E)-N-methyl-5-(3-(5-iso-propoxypyridin)yl)-4-penten-2-amine or pharmaceutically acceptable salts thereof, to the preparation of said compositions and the use of thereof in therapy.
WO2009087151A9 Polymorphic forms of moxifloxacin hydrochloride and processes for preparation thereof Polymorphic hydrate crystalline forms of Moxifloxacin hydrochloride were found, referred to hereinafter as polymorphic Form α1 and Form α2. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms, to pharmaceutical compositions comprising them, as well as their use.
WO2010083385A2 Compounds for reducing drug resistance and uses thereof This invention provides compounds capable of reducing drug resistance in a subject undergoing cancer treatment, methods using the compounds, compositions, and methods for identifying such compounds.
CN103393693A Pharmaceutical composition of ondansetron hydrochloride and dexamethasone The invention relates to a pharmaceutical composition of ondansetron hydrochloride and dexamethasone, and particularly relates to a combined application package comprising an ondansetron hydrochloride injection and an injection containing dexamethasone. When the combined application package is in use, the ondansetron hydrochloride injection and the injection containing dexamethasone are co-dissolved in normal saline, a Ringer's solution, 5% glucose injection and the like for intravenous infusion, so that a curative effect of stopping vomit can be increased.
CA2217551C Photoactivated hypericin and the use thereof The invention provides methods of using photoactivated hypericin compounds which, when photoactivated using visible or UV-A light, are useful for treating numerous diseases and disorders in mammals. The compounds of the invention are useful for inhibiting the proliferation and accumulation of mammalian leukocytes and for inducing apoptosis in mammalian leukocytes.
US20100256202 5,6-diaryl pyridines substituted in the 2- and 3-position, preparation thereof and therapeutic use thereof The invention relates to compounds corresponding to formula (I): In which Ar1, Ar2, Q, Y, Z, Alk′, k and m are as defined herein. The invention further relates to their preparations, intermediates therefor and their therapeutic uses.
CN102078612A Nasal in-situ gel containing mometasone furoate and H1 receptor antagonist The invention discloses nasal in-situ gel containing mometasone furoate and an H1 receptor antagonist. The nasal in-situ gel is prepared from mometasone furoate serving as an active ingredient and/or a hydrate of mometasone furoate, one or more H1 receptor antagonists, an environmentally-sensitive hydrophilic gel material, other pharmaceutically acceptable auxiliary materials and the balance of water.
EP1411919B1 (-)-olivil as antioxidant This invention relates to a pharmaceutical composition comprising an effective amount of (-)-Olivil together with or associated with an additive useful as an antioxidant; a process for isolating the (-)-Olivil from the pant Stereospermum Personatum and also relates to use of the active fraction (-)-Olivil as an antioxidant or free radical scavenger.
US7122214 Containing over 30 percent of total flavonoids; the naringin contained in the flavonoids is more than 30 percent Rhizoma Drynariae extract (RDE) is used as therapeutical agent or in the preparation for Osteoporosis, which is characterized in containing over 30 percent of total flavonoids. Furthermore naringin contained in flavonoids is more than 30 percent and less than 100 percent. The RDE is applied for the therapy of osteoporosis or used for producing drugs treating osteoporosis. And methods of extracting the same are also related.
CN102872008A Applications of Aphanamixoid A in medicaments for treating leukemia The invention relates to an application of Aphanamixoid A in preparing medicaments for treating leukaemia, belongs to the field of medicines, and relates to an application of Aphanamixoid A in preparing medicaments for treating leukaemia, an application of Aphanamixoid A in preparing medicaments for inhibiting multiplication of leukaemia cells and an application of Aphanamixoid A in preparing medicaments for inducing apoptosis of leukaemia cells. Aphanamixoid A is used for treating leukaemia through inhibiting multiplication of leukaemia cells and inducing apoptosis of leukaemia cells. The applicaiton of Aphanamixoid A in preparing medicaments for treating leukaemia, involved in the invention, is disclosed for the first time; the skeleton type is unusual; and meanwhile, the activity of Aphanamixoid A on inhibiting leukaemia cells is unexpectedly strong.
US20100062079 Polymorphisms predictive of platinum-coordinating complex induced ototoxicity Provided are methods, nucleic acids, and arrays for assessing the susceptibility of a subject to the development of ototoxicity in response to receiving one or more platinum-coordinating compounds, the method including determining the presence or absence of one or more polymorphisms, wherein the presence or absence of one or more such polymorphisms is indicative of susceptibility to the development of ototoxicity.
CN103432241A Chinese and Western external preparation for treating burns and scalds The invention discloses a Chinese and Western external preparation for treating burns and scalds. The preparation comprises antibiotic, distilled water, as well as Chinese angelica and garden burnet at a weight ratio of 1:(30-80):(30-50). A preparation method of a Chinese angelica and garden burnet equal extract comprises the steps of mixing and cooking the Chinese angelica and the garden burnet in the same parts by weight with the distilled water at a weight ratio of 1:13, and filtering and extracting juice, namely the Chinese angelica and garden burnet equal extract, 10 minutes after boiling. The Chinese and Western external preparation has the advantages that the preparation has the characteristics of no need of isolation and skin grafting, short treatment cycle, high cure rate, low possibility of infection, low probability of scars, lower treatment cost and the like; the probability of the scars is lower, and no pigmentation occurs after curing for second-third-degree burn and scald patients with burn and scald areas less than 50%. The medicine can inhibit great proliferation of fibroblasts, has functions of resisting local infection and promoting quick formation of skin islands in burnt sites, and achieves the purpose of quickly curing the burns.
WO2007071159A1 The use of anthraquinone derivatives for preparation of medicaments against influenza and “bird flu” viruse The use of anthraquinone derivatives for preparation of medicaments against influenza and 'bird flu' viruse is disclosed. Said anthraquinone derivatives comprise emodin, chysophanol, physcion, aloe emodin and rhein. Accordingly, emodin, chysophanol, physcion, aloe emodin and rhein as active ingredients may be used for preparation of medicaments against influenza and 'bird flu' viruse, the dosage forms of which are capsules, tablets, granules and injections.
US20080038369 Methods And Compositions For The Treatment Of Prolactin-Receptor Related Disorders The present invention provides methods and compositions for the treatment, diagnosis, prevention, or amelioration of one or more symptoms of a prolactin receptor-related condition, including, for example, a cancer such as breast cancer or prostate cancer, by administering a growth hormone-based prolactin receptor antagonist and zinc, or administering a growth hormone-based prolactin receptor antagonist to a tissue with an effective local concentration of zinc. The invention further provides pharmaceutical compositions of growth hormone-based prolactin receptor antagonists and zinc useful in the methods of the invention.
CN102783652A Preparation method of natural chromium powder sugar-reducing pill A natural chromium powder sugar-reducing pill is an invented up-to-date product special for treating diabetes at present; before the invention, a lot of products for treating diabetes are on the market, but no product is found to adopt a mineral trace element of chromium to treat diabetes; the product is prepared by chromium and a plurality of mineral vitamins. The product can supplement requirements for various nutritional components by the human body, and maintain physiological balance of the human body. The chromium element has the functions of blood sugar adjustment and stabilization, can reduce high blood sugar and increase low blood sugar, and thus maintain a normal level of the human blood sugar value.
US20110224290 Combine use of pterostilbene and quercetin for the production of cancer treatment medicaments The invention relates to the combined use of pterostilbene and quercetin for the production of cancer treatment medicaments. The in vitro growth of melanoma cells B16-F10 (B16M-F10) is inhibited (56%) by combined exposures of short duration (60 min/day) to PTER (40 μM)+QUER (20 μM) (˜average values of plasma concentrations measured within the first hour following the IV administration of 20 mg of each polyphenol/kg ˜). The combined intravenous administration of PTER+QUER (20 mg/kg×day) to mice inhibits (73%) the metastatic growth of melanoma B16M-F10 in the liver, a common site for metastasis development. The invention demonstrates that the combination of PTER+QUER inhibits the growth of malignant melanoma metastasis and prolongs the survival of the carrier host.
US20080279927 Non-Pegylated Long-Circulating Liposomes The present invention provides a long circulating non-pegylated liposomal doxorubicin hydrochloride composition for parenteral administration and a process for its preparation. The circulation time in Swiss albino mice is at least 25 times longer than conventional non-liposomal formulations. The non-pegylated liposomes are stable, exhibit low toxicity and have been found to be efficacious in different tumor models.
US7022315 Administering a thiol-based chemoprotectant agent intra-arterially for therapy and prophylaxis of side effects of cytotoxic cancer therapy for tumors located in the brain, head or neck A method of administration of a thiol-based chemoprotectant agent including NAC (N-acetylcysteine) and STS (sodium thiosulfate) that markedly affects biodistribution and protects against injury from diagnostic or therapeutic intra-arterial procedures. A method for treating or mitigating the side effects of cytotoxic cancer therapy for tumors located in the head or neck and brain tumors. The thiol-based chemoprotectant agent is administered intra-arterially with rapid and first pass uptake in organs and tissues other than the liver.
CN1611603A Novel DNA fragment and its inhibition from tumour This invention involves one new DNA fragment and its control of cancer and its expression albumen, especially the DNA fragment named as TSF395 and its expression albumen, which can be used to inhibit the growth of tumor cells.
CN101781320A Cephalosporin derivative containing pyridinium ions The invention belongs to the technical field of medicine, particularly relates to a cephalosporin derivative containing pyridinium ions, pharmaceutically acceptable salts and an easily hydrolysable ester or an isomer thereof as shown in a general formula (I), wherein meanings of R1, R2, R3, R4, R5, R6,X and n are defined as the specification. In addition, the invention also provides preparation methods of the compounds, medical compositions containing the compounds, and application of the compounds in preparing medicaments for treating and/or preventing infectious diseases.
CN101317956A Pharmaceutical composition for preventing birth defection and improving memory The present invention provides a medicine compound for preventing birth defects and improving memory. The compound contains largehead atractylode, polygonatum, complex vitamin B, vitamin D, macroelements of Ca, K and Mg, and microelements of Zn, Se, Fe, Cr, Cu, Mo, I and Mn. The medicine compound is mainly suitable for progestational women, pregnant women and nannies and effective for preventing birth defects and improving memory. In addition, the medicine compound has the efficacy of healthcare and invigoration and does not generate any side effect even in long-term application.
US7569598 Isomerization; crystallization The present invention relates to a process for the enrichment of the R,R- or S,S-configured glycopyrronium isomers and their thienyl derivatives having the R,S or S,R configuration.
US20050112675 Polypeptides gene expressed in fat tissue ; measurement concentration; using antibodies The present invention provides polypeptides which are predominately expressed in visceral adipose tissue which can be used as markers for the measurement of the levels of visceral adipose tissue in a subject. The invention also provides methods for the measurement of the levels of visceral adipose tissue by obtaining a biological sample and detecting and/or measuring the increase of one or more polypeptides as disclosed herein. Screening methods relating to agonists and antagonists of the specific polypeptides disclosed herein are provided. Antibodies may also be raised against these polypeptide markers for the detection and/or treatment of metabolic syndrome related comorbidities.
CN103450208A Antibacterial compound as well as preparation method and application thereof The invention discloses an antibacterial compound as well as a preparation method and an application thereof. The antibacterial compound is shown in a formula I or II. Experiments show that the antibacterial compound is brand new in structure, has better antibacterial activity and is applicable to research of an antibacterial lead compound or preparation of an antibacterial drug.
CN101822683A Medical care application of L-arabinose composition The invention belongs to the field of biological medicaments and health-care products, and relates to application of L-arabinose in preventing obesity and reducing weight, in particular to the application of the L-arabinose. The application of the L-arabinose composition is that the composition can effectively prevent increase of fat index in a human body caused by a high-sugar, high-fat and high-cholesterol diet, reduce the large amount of fat having been accumulated in the human body and reduce the weight through oral application.
EP2299824A1 Pyrazole derivatives useful as inhibitors of faah The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer disease, and Parkinson's disease
US8263582 Administering two separate dosage forms of a topically active corticosteroid or a pharmaceutically active salt thereof for therapy ofinflammatory bowel disease and sufficient to reduce or eliminate side effects A method of administration of an oral pharmaceutical product to patients suffering from inflammatory disorders of the gastrointestinal tract comprises orally administering to the patient at least two different dosage forms of a therapeutically effective amount of a topically active corticosteroid, such as beclomethasone dipropionate (BDP).
CN102947311A 3-oxo-3,9-dihydro-1h-chromeno[2,3-c]pyrroles as glucokinase activators The present invention provides novel compounds of formula (I), wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
WO2008135826A3 2 -pyridine carboxamide derivatives as sodium channel modulators The present invention relates to compounds of the formula (I): (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
WO2010149384A3 Hybrid molecules made of lipids and lipid-analogous compounds and use thereof as pharmaceutical or cosmetic preparation The invention relates to hybrid molecules made of two lipids or lipid- analogous compounds which are linked to each other via their lipophilic end. The hybrid molecules thereby have at least one hydrophilic group at their hydrophilic end for increasing the hydration shell of the hybrid molecule. The hybrid molecules according to the invention can be used as pharmaceutical or as a cosmetic preparation.
CN101632459B Application of pectic acid oligosaccharide in preparing health-care product treating gastric ulcer The invention relates to an application of pectic acid oligosaccharide in preparing a health-care product treating gastric ulcer. The invention adopts the technical scheme that firstly, pectin is dissolved in water, and a pectin decomposer is prepared by a decomposition reaction; the pectin decomposer is processed by using a hollow fibre film or a ceramic filtration film, an oligosaccharide mixture with the molecular weight of 200-6000 daltons is processed and recovered by using a nano filtration film after an oligosaccharide mixture with the molecular weight being below 6000 daltons is recovered, and the pectic acid oligosaccharide with the superposition degree of 2-20 is obtained by the chromatographic separation of a Bio-gel P-2 gel column and/or a Sephadex G-25 gel column or the filtration of DEAE-Sephadex A-25 anion exchange resin. The prepared pectic acid oligosaccharide and auxiliary materials are matched to prepare health-care products with various forms and components for treating the gastric ulcer. The invention adopts a congeneric theory of medicines and foods, has no toxic or side effect and can be taken for a long time. By verification, the invention has obvious curative effect to sour burning type gastric ulcer.
WO2007005887A3 Androgen receptor modulator compounds, compositions and uses thereof Provided herein are compounds that selected from Formula I, Formula Ia, Formula II, Formula IIa, Formula IIb, Formula III, Formula IV, Formula V and Formula VI: bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
US20100239599 Vaccine Peptide Combinations Against Cat Allergy The present invention relates to compositions comprising peptides for preventing or treating allergy to cats, and in particular to optimal combinations of peptides.
CN101574341A Oral solid medicine composition containing ropinirole The invention discloses an oral solid medicine composition containing ropinirole. The oral solid medicine composition comprises a medicine containing part and hollow white granules, wherein the medicine containing part contains ropinirole and pharmaceutically acceptable carriers, and the hollow white granules contain no ropinirole and are formed by mixing pharmaceutically acceptable carriers. Theoral solid medicine composition can be prepared with simple process, has better uniformity of preparation content and stability and can be used for treating parkinson disease (PD).
US20070225356 Preventive and/or Therapeutic Agent for Chronic Sinusitis The present invention provides a preventive and/or therapeutic agent and the like for chronic sinusitis, which comprises, as an active ingredient, a dibenzo[b,e]oxepine derivative represented by formula (I): (wherein R1, R2, and R3 may be the same or different and each represents a hydrogen atom or lower alkyl, and m and n may be the same or different and each represents an integer of 1 to 4) or a pharmaceutically acceptable salt thereof.
US20110002981 MCPIP Protection Against Cardiac Dysfunction Disclosed herein are methods and compositions of treating a patient at risk of experiencing sepsis induced cardiac dysfunction. In exemplary examples, the method involves elevating MCPIP levels in a patient in need. Elevating MCPIP levels may involve direct administration (e.g. delivery of protein) or indirect administration (e.g. delivery vehicle capable of increasing expression of MCPIP).
US20070281926 Rectal Composition A viscous or gellous pharmaceutical composition for the treatment of constipation by rectal administration comprises a polar lipid component, a polyvalent alcohol component, water, and optionally an oily triglyceride. Also disclosed is a compressible device filled with a single dose of the composition and a method for its manufacture; a method of treating constipation, comprising rectal administration of a constipation-dissolving amount of the composition; and a method of manufacture of a medicament for treating constipation comprising the composition of the invention.
CN100998860A Troxerutin cerebroprotein hydrolysate sodium chloride injection liquid An injection for treating cerebral thrombosis, cerebral infarction, cerebral spasm, cerebral dysfunction, obliteration syndrome, arteriosclerosis, thrombophlebitis, etc is prepared from troxerutin, cerebroprotein hydrolyzate, sodium chloride and the water for injection. Its preparing process is also disclosed.
US20080161321 Use of Renin Inhibitors in Therapy The present is directed to a method for the prevention of, delay progression to or treatment of a condition or disease selected from diabetes type 2 (associated with or without hypertension), severe hypertension, PH, malignant hypertension, isolated systolic hypertension, familial dyslipidemic hypertension, endothelial dysfunction (with or without hypertension), survival post-MI, increase of formation of collagen and other extracellular matrix proteins, restenosis after stenting, PVD including PAD and peripheral venous disorders, CAD, morbidity, mortality, cerebrovascular diseases, metabolic disorder (Syndrome X), AF, renoprotection, reduction of proteinuria, renal failure, glomerulonephritis, nephrotic syndrome, renal fibrosis, AIN, ATN, acute tubulo-interstitial nephritis, PKD, vascular inflammation, rennin secreting tumors, vasculitides or closure, restenosis of dialysis access grafts comprising administering a compound of formula (I) or a pharmaceutically acceptable salt thereof alone or in combination with another active ingredient.
US20110275681 Novel solid forms of epalrestat The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic.
CN102002132A Improvement on method for preparing complex of polyvinylpyrrolidone grafted with natural polymer or water-soluble derivate thereof and iodine derivate The invention provides improvement on a method for preparing complex of a polyvinylpyrrolidone copolymer grafted with a natural polymer or a water-soluble derivate thereof and an iodine derivate. The effective iodine content in the complex of the graft copolymer of the natural polymer or the water-soluble derivate thereof and iodine, the stability of the complex iodine and the freezing and drying working efficiency of the concentrate of the complex or the compounds thereof are improved by improved means of compounding a long-chain alkyl anion surfactant or a long-chain alkyl nonionic surfactant and the polyvinyl-containing natural polymer or the water-soluble derivate-grafted polyvinylpyrrolidone chain segment, compounding iodide and iodine, and replacing ethanol with an organic solvent with a high freezing point, high volatility and capability of dissolving in water and dissolving the iodine to a certain degree to improve the freezing and drying speed of the concentrate the complex of the graft copolymer and the iodine or compounds thereof, and the like.
WO2012000306A1 Phenyl nitrone compounds containing stilbene segment and use thereof Phenyl nitrone compounds containing stilbene segment and pharmaceutically acceptable salts thereof are provided. The above compounds can be used for treating cancer and also can be used as neuroprotective agent. Preparation method of the above compounds, pharmaceutical compositions comprising the above compounds and their use in the preparation of anti-tumor medicines are also provided.
US20110212985 Naltrexone Long Acting Formulations and Methods of Use The inventions described herein arose from unexpected discoveries made during clinical trials with a long acting formulation of naltrexone. As such, the invention includes a method for treating an individual in need of naltrexone comprising the step of parenterally administering a long acting formulation comprising naltrexone and to the use of naltrexone in the manufacture of medicaments for use in such methods.
WO2010116282A1 4, 5-dihydro-lh-pyrazole compounds and their pharmaceutical uses Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
EP1612225A1 Modified acacia and use thereof The present invention aims to provide modified gum arabic having an increased total dietary fiber content and use thereof. The modified gum arabic of the present invention, which is obtained by heating gum arabic, has a total dietary fiber content (determined by AOAC method) of not less than 90%, and preferably has a weight-average molecular weight of not less than 1,000,000. This modified gum Arabic is usable as a dietary fiber material or an additive for enriching dietary fiber to be used in foods, drinks and medicines. Therefore, the present invention provides foods, drinks or medicines containing the above-described modified gum Arabic as dietary fiber material or an additive for enriching dietary fiber.
CN103083251A Application of tanshinone IIA-polyactic acid/hydroxyacetic acid microsphere to preparation of antitumor drugs The invention discloses an application of a tanshinone IIA-polyactic acid/hydroxyacetic acid microsphere to the preparation of antitumor drugs. The microsphere is prepared by drying oil-in-water type emulsion, wherein the oil phase is dichloromethane solution of a polyactic acid/hydroxyacetic acid copolymer and the water phase is the water solution of polyvinyl alcohol. The drug content of tanshinone IIA in the microsphere is 1-10% and the entrapment efficiency is 60-90%. The particle size range of the microsphere is 30-200mm. The tanshinone IIA-polyactic acid/hydroxyacetic acid microsphere provided by the invention is suitable for interventional therapy of liver cancers, has a good liver tumor peripheral vascular thrombosis function, has an effective thrombosis time of 7-60 days, can be distributed in tumor tissues in a targeted manner, slowly release drugs, increase the local concentrations of the drugs, prolong the drug metabolism time, obviously inhibit animal liver tumor growth and prolong the animal lifetime and can inhibit expressions of a human hypoxia inducible factor 1alpha and a vascular endothelial growth factor and reduce the tumor tissue microvessel density after thrombosis.
WO2011140334A3 Compounds, methods of making or identifying compounds, and uses thereof The present invention provides various compounds, compositions, and methods. In some embodiments, provided compounds have activity as, for example, inhibitors of protein translation.
US20120329842 Small molecule compounds as broad-spectrum inhibitors of metallo-beta-lactamases The present invention concerns methods and/or compositions for treatment and/or prevention of bacterial infection wherein the bacteria has at least one metallo-β-lactamase. The bacteria are provided with an inhibitor of the metallo-β-lactamase, for example in conjunction with an antibiotic that targets the bacteria. The bacteria may be a drug-resistant strain or susceptible to becoming a drug-resistant strain. In specific embodiments, the bacteria is Pseudomonas or Acinetobacter spp.
EP2265581A1 Compounds having crth2 antagonist activity Compounds of general formula (I) W is chloro or fluoro; Z is a -SO2YR1 group wherein R1 is C3-C8 heterocyclyl, aryl or heteroaryl any of which may optionally be substituted with one or more substituents selected from halo, -CN, -C1-C6 alkyl, -SOR3, -SO2R3, -SO2N(R2)2, -N(R2)2, -NR2C(O)R3, -CO2R2, -CONR2R3, -NO2, -OR2, -SR2, -O(CH2)POR2, and -O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, -C1-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, -C1-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; Y is a straight or branched C1-C4 alkylene chain; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
CN103638526A Preparation for purifying blood as well as preparation method and application thereof The invention relates to a preparation for purifying blood as well as a preparation method and an application thereof, and belongs to the technical field of medicines. The preparation for purifying blood disclosed by the invention is a solid-state preparation or a liquid-state preparation, and contains an acid-base regulator; the acid-base regulator is a mixture of one or two of L-malic acid or DL-malic acid. By adopting the preparation for purifying the blood, the defects of currently used acid-base regulators are overcome, and the preparation has good biocompatibility, and is widely applied to the aspects of manufacturing and production and clinical treatment.
US20050125039 Treatment of hepatitis C using hyperthermia The invention provides a method of treating a patient infected with hepatitis C virus (HCV) comprising raising the core temperature of the patient and then returning the core temperature of the patient to normal at least one time, wherein the core temperature is raised to a temperature range and a duration sufficient to reduce or eliminate the patient's viral load of HCV.
WO2007009655A1 1,4-benzothiazepine 1,1-dioxide derivative, process for its preparation, medicaments comprising this compound, and use thereof as a hypolipidaemic The invention relates to the compound of the formula (A) and also to its physiologically acceptable salts. The compound is suitable as, for example, a hypolipidaemic.
EP2447264A1 N-substituted-cyclic amino derivative The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is -N(R1b)-, G2 is -CO-, G3 is -C(R1c)(R1d)-, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c, and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.
US8048454 Methods and compositions related to regulation of cytokine production by glycogen synthase kinase 3 (GSK-3) This invention relates generally to a method of treating inflammation and associated diseases and disorders by administering an agent that inhibits glycogen synthase kinase 3 activity.
WO2012157746A1 Therapeutic drug for autoimmune disease The present invention provides a screening method for a preventive or therapeutic agent for an autoimmune disease, comprising evaluating agonist activity or antagonist activity of a test compound on a lysophosphatidylserine receptor using P2Y10 or GPR174.
US20060083784 Amorphous pharmaceutical compositions The present invention is directed to use of electrospinning, i.e. the process of making polymer nanofibers from either a solution or melt under electrical forces, to prepare stable, solid dispersions of amorphous drugs in polymer nanofibers. The present invention is also directed to the process of making solid dispersions of amorphous forms and compositions of rosiglitazone and its pharmaceutically acceptable salts.
EP2714086A1 Polyphenol composition for preventing or treating atherosclerosis This invention relates to the provision of an oral composition for preventing or treating atherosclerosis. Thus in one of the invention, an oral composition for preventing or treating atherosclerosis is provided, the composition comprising curcumin and a composition containing as its main component proanthocyanidin oligomer to which a substance having a phloroglucinol ring structure or resorcinol ring structure has been bonded, which is obtainable by heating plant materials comprising proanthocyanidin polymer or aqueous extract thereof comprising proanthocyanidin polymer, with a substance having a phloroglucinol ring structure or resorcinol ring structure in an acidic aqueous solution.
WO2008148892A2 Mc- i r, mc-2 r, and mu opioid receptors modulation The invention concerns active substances modulating the expression of the receptors of the products of the POMC gene (MC-IR, MC-2R, and the μ opioid receptor), and possibly modulating the expression of POMC in cutaneous cells, notably to modulate the proliferation and differentiation of epidermal cells in order to re-epithelial, maintain innervation, irrigate the skin, or restore normal pigmentation, or to fight against aging, or to modulate pigmentation independently or not of cutaneous aging. The invention also concerns a method of screening such active substances.
WO2011009890A3 Use of azabicycloalkyl derivatives or pyrrolidine - 2 - one derivatives for the treatment or prevention of ataxia The invention concerns the use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives for the treatment, prevention or delay of progression of ataxia.
CN102805730A Ceramide liposome and preparation method and application thereof The invention relates to ceramide liposome and a preparation method and application thereof. The ceramide liposome comprises a therapeutically effective amount of active component and a lipid bilayer film, and is characterized in that the ceramide liposome comprises 0.5 to 20 weight parts of ceramide used as the active component and 10 to 350 weight parts of the lipid bilayer film, wherein the lipid bilayer film comprises the following components in part by weight: 5 to 100 parts of phospholipid substance, 0.5 to 10 parts of cholesterol, 0 to 100 parts of surfactant, 0 to 20 parts of additive and 0.5 to 10 parts of organic solvent. The preparation method comprises the following steps of: fully dissolving the ceramide, the phospholipid substance, the cholesterol and the additive in the organic solvent, dissolving the surfactant in a dispersion medium to prepare the ceramide liposome, and reducing the average particle size of the prepared ceramide liposome to less than 500nm to ensure that the particle sizes are uniformly distributed. The invention also discloses new application of the ceramide liposome to cancer therapy.
US20060035909 2,6,9-trisubstituted 8-azapurines such as 2-(4-aminocyclohexylamino)-6-benzylamino-9-isopropyl-8-azapurine, used as cyclin-dependent kinase inhibitors, in the treatment of skin disorders, viral infections, cancer, arthritis, lupus, diabetes, multiple sclerosis, restenosis, polycystic kidney disease, gout The present invention relates to a compound of formula I, or a pharmaceutically acceptable acid salt thereof. The invention further relates to the use of said compounds in the treatment of hyperproliferative skin disorders, viral infections, cancer, rheumatoid arthritis, lupus, type I diabetes, multiple sclerosis, restenosis, polycystic kidney disease, graft rejection, graft versus host disease and gout, or for psoriasis, parasitoses such as those caused by fungi or protists, or Alzheimer's disease. Further aspects of the invention relate to the use of such compounds in the inhibition of cell proliferation, in the induction of apoptosis, to modulate the activity of adrenergic and/or purinergic receptors or to suppress immunostimulation. The invention also relates to the use of 2,6,9-trisubstituted 8-azapurines in maintaining mammalian ooctyes at the germinal vesicle stage.
CN102657682A Semen preparation method for improving sow fertility The invention discloses a semen preparation method for improving sow fertility in the technical field of propagation of livestock. The semen preparation method comprises the following steps of: filtering and screening collected semen of a boar; removing the semen; diluting with a diluting agent; adding vitamin E into the mixed solution; uniformly mixing and then storing in storage environment of 16-17 DEG C; adding cloprostenol before artificial insemination; and uniformly shaking for later use. The semen preparation method has the beneficial effects that: an artificial insemination method is adopted by the semen mixed solution obtained by the method; after the semen is introduced into the uterus of a sow, the conception rate of the sow can be increased, and 12-13 piglets can be born by the sow; and compared with the conventional artificial insemination and propagation in the prior art, 0.5-1.5 piglets are increased, and obvious economic benefit is achieved.
CN102846634A Inhalant containing N-acetyl-L-cysteine and budesonide and preparation method thereof The invention relates to an inhalant containing N-acetyl-L-cysteine and budesonide and preparation method thereof. The inhalant is composed of budesonide and N-acetyl-L-cysteine as the active ingredients, and one or more pharmaceutical adjuvants suitable for inhalation drug delivery.
US20120003177 Curcumin-containing polymers and water-soluble curcumin derivatives as prodrugs of prodrug carriers Curcumin, a polyphenol extracted from the rhizome turmeric, has been polymerized to produce a polymer material having a backbone of one or more repeating structural units, at least one of which comprises a curcumin monomer residue. These curcumin-containing polymers have a wide range of pharmacological activities, including, among others antitumor, antioxidant, antiinflammatory, antithrombotic and antibacterial activities. Certain species of these polymers have exhibited remarkable antitumor activity. Water-soluble curcumin derivatives and their use as prodrugs and prodrug carriers are also disclosed.
US7265154 Valproic acid and derivatives thereof as histone deacetylase inhibitors The present invention relates to the use of the drug valproic acid and derivatives thereof as inhibitors of enzymes having histone deacetylase activity. The invention also relates to the use of those compounds for the manufacture of a medicament for the treatment of diseases which are associated with hypoacetylation of histones or in which induction of hyperacetylation has a beneficial effect for example by induction of differentiation and/or apoptosis in transformed cells.
CN101553486A Oxadiazole and thiadiazole compounds and their use as nicotinic acetylcholine receptor modulators This invention relates to oxadiazolyl and thiadiazolyl derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
US20110313035 Polymorphs of darunavir The present invention provides novel solvated forms of darunavir and processes for there preparation. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form.
US20120232149 Solid pharmaceutical compositions containing pregabalin A solid pharmaceutical composition containing pregabalin is described. The composition includes a matrix forming agent and a swelling agent and is suitable for once daily oral administration. Exemplary matrix forming agents include mixtures of polyvinyl acetate and polyvinylpyrrolidone, and exemplary swelling agents include cross-linked polymers of polyvinylpyrrolidone.
DE102006011510A1 Combination pills for contraception and therapy, contain gestagen and phytoestrogen, and ensure good estrogen supply without causing bleeding New combination pills (A), designated 'biopills', contain a gestagen (I) and a phytoestrogen (II). Alternatively (I)/(II) combinations are formulated in dosage forms other than pills, e.g. implant or depot formulations. - ACTIVITY : Antifertility. - MECHANISM OF ACTION : Gestagen; Estrogen.
EP2398475A1 Pharmaceutical preparation and delivery system The present invention relates to unique delivery systems and the use of an imidazobenzodiazepine derivative, such as flumazenil either alone or in combination with other receptor antagonists in the treatment of disease or medical disorders.
WO2007120102A1 New substituted oxindole derivatives The present invention relates to new compounds of formula (I). Wherein R1 is hydrogen or hydroxyl, Q is N or N+O- with the proviso that when R1 is hydrogen then Q is N+O- and when R1 is hydroxy then Q is N, as a free base or a pharmaceutically acceptable salt thereof, in an essentially pure and isolated form, pharmaceutical formulations containing said compounds, to the use of said active compounds in therapy, and particularly to GSK3 related disorders, and processes for their preparations as well as new intermediates.
US20080176950 Treatments Using Venlafaxine This; invention provides a method of treating obesity, generalized anxiety disorder, post-traumatic stress disorder, late luteal phase dysphoric disorder (premenstrual, syndrome), attention deficit disorder, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa or Shy Drager Syndrome in a: mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine of the following structural formula: in which A is a moiety of the formula where the dotted line represents optional unsaturation; R1 is hydrogen or alkyl; R2 is alkyl; R4 is hydrogen, alkyl, formyl, or alkanol; R5 and R6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy; R7 is hydrogen or alkyl; and n is 0, 1, 2, 3, or 4; or a pharmaceutically acceptable salt thereof:
EP2146951B1 Novel rar receptor agonist ligands and use thereof in human medicine and cosmetics The invention relates to compounds having general formula (I), compositions containing same, the preparation methods thereof and the use of same in pharmaceutical compositions intended for use in human or veterinary medicine or cosmetic compositions.
US20110269839 Anti-snoring composition containing a termogelling polymer The invention relates to a composition for treating and/or preventing snoring, comprising at least one thermogelling polymer that includes water-soluble units as well as units having a lower critical demixing temperature in water. Said composition has the specific feature of being liquid in the packaging thereof and becoming a gel upon contacting mucus membranes at 37° C. Thermogelling makes it possible to precisely target the area to be treated while avoiding any running or migration of the material, and makes the sprayed composition difficult to wash off, thus increasing the duration of the presence thereof in the treatment area.
US20070015737 Compounds for inhibiting diseases and preparing cells for transplantation Methods and compositions which are useful in the treatment of amyloidosis. In particular, methods and compositions are provided for inhibiting, preventing and treating amyloid depositions, e.g. in pancreatic islets, wherein the amyloidotic deposits are islet amyloid polypeptide (IAPP)-associated amyloid deposition or deposits. The methods of the invention involved administering to a subject a therapeutic compound which inhibits IAPP-associated amyloid deposits. Accordingly, the compositions and method of the invention are useful for inhibiting IAPP-associated amyloidosis in disorders in which such amyloid deposition occurs, such an diabetes. The invention also provides a process for the preparation of cells suitable for transplantation into a mammal, which cells are capable of forming fibrils, said process comprising contacting the cells with an inhibitor of fibril formation. In particular the process prepares cells for use in a method of treating diabetes. Also provided are a culture medium comprising the inhibitor and cells for transplantation.
CN101757599B Medicinal granules comprising brown sugar, Colla corii Asini, Cornu cervi Pantotrichum, ginseng, clove, costus root, red jujube and tea The invention provides medicinal granules comprising brown sugar, Colla corii Asini, Cornu cervi Pantotrichum, ginseng, clove, costus root, red jujube and tea, which are prepared by the following raw materials in parts by weight: 10 to 20 parts of brown sugar, 10 to 20 parts of gordon euryale seed, 1 to 5 parts of red sage root, 1 to 5 parts of Colla corii Asini, 1 to 5 parts of Cornu cervi Pantotrichum, 5 to 10 parts of lotus seed, 1 to 5 parts of ginseng, 1 to 5 parts of clove, 1 to 5 parts of costus root, 1 to 5 parts of motherwort, 1 to 5 parts of angelica, 1 to 5 parts of aconite, 1 to 5parts of Rhizoma zingiberis, 3 to 8 parts of red jujube, 1 to 5 parts of puer tea and 1 to 5 parts of Radix rehmanniae Preparata. The product is scientifically prepared according to the physiologicalcharacteristics of the majority of women, the raw materials are easy to buy and store, and the drinking is convenient; the product has remarkable effects for dysmenorrhea of women and alleviating pain of patients, can invigorate spleen and replenish qi, and alleviate pain when being eaten regularly, and is an essential nutrition food for women in daily life; and therefore, the promotion value is very good.
CN102146040A 2-(4-Chlorophenoxy)-2-methylpropionic acid methoxyphenyl propionate compound and synthesis method thereof The invention discloses a 2-(4-Chlorophenoxy)-2-methylpropionic acid methoxyphenyl propionate compound which can be used for reducing cholesterol and low-density lipoprotein in a hyperlipidaemia model. By structural confirmation, the compound has the following structure that a synthesis method of the compound comprises the following steps of: taking 2-(4-Chlorophenoxy)-2-methylpropionic acid (1mol to 0.1mol), tetrahydro furan (100ml to 20ml), 1,3-dicyclohexylcarbodiimide (1mol to 0.1mol) and vanillin pyridine solution (1mol to 0.1mol); performing a reaction for 6 hours at a temperature of 10 DEG C to 30 DEG C; pouring reaction solution into water to obtain a crude product; carrying out recrystallization on the crude product by ethanol to obtain white solid; then adding malonic acid (1mol to 0.1mol) and pyridine (1mol to 0.1mol); and performing a reaction for 10 hours at a temperature of 100 DEG C to 120 DEG C to obtain white solid serving as the compound product. The compound has the yield of 85 percent.
CN1582919A Preparation of medicines for reducing blood sugar and triglyceride from hippophae rhamnoides flavone A medicine in the form of tablet or capsule for decreasing blood sugar and triglyceride is prepared from seabucklthorn flavone and the auxiliary chosen from microcrystalline cellulose, hydroxypropyl cellulose, hydroxymethyl amylosodium, talc powder, gelatin, glycerine, water and refined vegetable oil.
CN1903212A Application of methyl astragalin for preparing medicines An application of the astragaloside A in preparing the medicines for preventing and treating the immunomediation-type chronic inflammation, such as rheumatoid arthritis and/or lupus erythematosus, is disclosed.
WO2007029156A3 Isoindoledione derivatives as adrenergic receptor antagonists Provided are isoindoledione derivatives, which can be used of treating a disease or disorder mediated through αla and/or α1(1 adrenergic receptors. Compounds disclosed herein can be used of treating benign prostatic hyperplasia (BPH) and related symptoms thereof, lower urinary tract symptoms (LUTS) associated with or without BPH. Processes for the preparation of described compounds, pharmaceutical compositions thereof, and methods of treating BPH and related symptoms thereof, LUTS associated with or without BPH are also provided.
CN102451447A Manufacturing method of medicament for treating chilblain The invention relates to a manufacturing method of a medicament for treating chilblain. Drugs of angelica sinensis, safflower carthamus, ricepaper pith, rhizoma zingiberis and root of common peony are immersed in 95% alcohol and filtered; slag is removed; and medical soup is filled into a bottle and can be slightly applied to an affected part by cotton. The medicament of the invention is suitable for non-festered chilblain, has substantial effect, and is easily prepared, convenient for usage and a good approach for treating and preventing chilblain.
CN102100696A Bone joint maintenance composite containing dimethyl sulfone The invention relates to composition of a composite containing dimethyl sulfone and a preparation method of dosage form thereof, belonging to the fields of medicines, health-care products and food. The composite containing dimethyl sulfone mainly comprises dimethyl sulfone, glucosamine and salts thereof, adhesive, excipient, addictive and the like. The bone joint maintenance composite containing dimethyl sulfone is characterized in that dimethyl sulfone is a necessary key component; the adhesive is arabic gum or sodium carboxymethylcellulose (CMC-Na); and the used dosage form of the composite containing dimethyl sulfone can be granules, capsules and tablets. The composite containing dimethyl sulfone can be applied to clinical treatment of bone joint inflammation and bone joint cartilage and anadesma, and daily maintenance of conjunctive tissues and connective tissues.
CN103120684A Application of Aphanamixoid A in medicine for treating endometrial carcinoma The invention discloses an application of Aphanamixoid A in preparation of a medicine for treating endometrial carcinoma, and belongs to the technical field of new application of the medicine. The Aphanamixoid A has outstanding inhibiting effect on the growth of human endometrial carcinoma cell strains ISK and RL95-2 through in-vitro MTT antineoplastic activity evaluation. Thus, the Aphanamixoid A can be used for preparing the medicine for resisting the endometrial carcinoma and has good development and application prospect; and the application of the Aphanamixoid A in preparation of the medicine for treating the endometrial carcinoma is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on endometrial carcinoma cells is inconceivably high.
WO2011069334A1 Cdk5 inhibitors and therapeutic uses thereof Natural occurring inhibitors of cyclin-dependent protein kinase 5 (Cdk5), isolated from the root of Rhodiola rosea are structurally different from the known Cdk inhibitors. They show selectivity among different Cdks and efficacy to inhibit Cdk via a mixed-type of inhibition, which should lead to less toxicity and side-effects. They are useful in preventing and treating diseases and disorders associated with aberrant Cdk5 activities, such as acute and/or chronic pain, neuropathic pain, diabetes mellitus, cancer, neurodegenerative diseases and neuropathological disorders.
CN101375845B Podophyllotoxin external-use formulation prescription for treating pointed condyloma and herpes genitalis, dosage form series and preparation method The invention discloses a podophyllotoxin preparation formula for external use for the treatment of condyloma acuminatum and genital herpes, a series of formulations and a preparation method, and belongs to the field of pharmacy. The weights or the volumes of all the ingredients of the formula of 100ml of the podophyllotoxin preparation for external use are as follows: 0.5g of podophyllotoxin, 20ml-80ml of main solvent, 1ml-3ml of penetration enhancer 1, 0.5g-2.5g of penetration enhancer 2, 20ml-80ml of cosolvent and 0.03-0.5g of preservative. The podophyllotoxin preparation for external use has the advantages that the types and the amount of excipients and the proportion of main drugs are reasonable, the drug administration is carried out by a liniment, a spray or other formulations which are applicable to the external use, the main drug can be rapidly absorbed by the horny layer and the epidermis, the efficacy is significant, the local toxicity or side effects are small, the skin acute toxicity is very low, and the podophyllotoxin preparation has no irritation and weak allergy and does not hinder the skin normal functions; the podophyllotoxin preparation has no systemic toxicityor side effects, thereby being safe and effective. The preparation prepared by the formula has the advantages of good appearance, moderate viscosity, easy coating, spraying drug administration, feasible process, controllable quality, simple preparation process, and suitability for industrial batch production.
US20090075953 Deuterium-enriched ed-71 The present application describes deuterium-enriched ED-71, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2014100700A1 Cytoprotective derivatives of avicin d and methods of making and using thereof Disclosed herein are cytoprotective derivatives of avicin D of formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising these derivative compounds. Methods and intermediates useful for making the derivatives, and methods of using the derivatives and compositions thereof, including for the treatment of cancer, are also provided.
CN102875529A Dabigatran derivatives and preparation method thereof The invention relates to Dabigatran derivatives and pharmaceutically acceptable salts thereof, which are shown in a general formula I, a preparation method for the derivatives in the formula I, medical compositions comprising the compounds as active ingredients, and use of the compounds and the medical compositions as thrombin inhibitors. In the formula I, R1 and R2 are respectively defined in the specifications.
WO2005032561A1 INVENTION RELATING TO FUNCTION OF HIV-Vpr It has been elucidated that HIV-1 Vpr protein has the function of controlling the splicing of HIV-1 mRNA and that the action thereof leads HIV-1 to the process of replication and multiplication, and the invention is based on the elucidation. There is provided a pharmaceutical composition for inhibiting the multiplication of HIV-1, characterized in that Vpr protein is inhibited, or its expression is suppressed. There is further provided a method of screening a substance capable of inhibiting the multiplication of HIV-1 characterized in that Vpr protein is inhibited.
WO2012032541A1 "adefovir dipivoxil pseudopolymorph" The present invention provides novel pseudopolymorph of Adefovir dipivoxil, and process for the preparation thereof. The present invention specifically relates to Adefovir dipivoxil formic acid solvate.
WO2008080064A1 Synthetic lipophilic inositol glycans for treatment of cancer and glucose-metabolism disorders The present intervention related to materials and methods for the synthesis of lipophilic inositol glycan compounds, and salts, solvates and physiological functional derivatives thereof, and their use for the treatment of cancer and glucose-metabolism disorders, such as, for example, diabetes, obesity and metabolic syndrome.
EP2573072A1 Indenoquinolone compound, preparation method and use thereof An indenoquinolone compounds of Formula (A) is disclosed, wherein the definition of each group is described in the description. These compounds may specifically inhibit topoisomerase I, and they have good activities against many kinds of human tumor cells, such as lung cancer, colon cancer, breast cancer, liver cancer and the like. They can be used in the manufacture of antitumor drugs. The method for preparing the compound of formula (A), and pharmaceutical compositions containing such compounds and the use in the manufacture of antitumor drugs are also disclosed.
US7468361 For therapy of skin conditions selected from the group consisting of dermatitis, eczema, keratosis, lack of skin firmness, wrinkles, lack of dermal hydration and insufficient sebum secretion Biologically active 19-nor vitamin D analogs substituted at C-2 in the A-ring with an ethylidene or an ethyl group. These compounds have preferential activity on mobilizing calcium from bone and either high or normal intestinal calcium transport activity which allows their in vivo administration for the treatment of metabolic bone diseases where bone loss is a major concern. These compounds are also characterized by high cell differentiation activity.
US20090215755 Use of a pyrazole derivative for preparing medicinal products that are useful in the prevention and treatment of dyslipidaemias and of diseases related to dyslipidaemias and/or to obesity Use of a pyrazole-derived compound that is an antagonist for cannabinoid CB1 receptors, alone or combined with another active principal, for preparing medicinal products that are useful in the prevention and treatment of dyslipidemias and of diseases related to dyslipidemias and/or to obesity, such as metabolic syndrome, cardiovascular risks and hepatic diseases.
EP1501493B1 Use of epa and dha in secondary prevention of strokes The invention is directed to the use of the n-3 PUFA EPA and/or DHA in the preparation of an oral medicament for preventing cerebral damage in patients having symptoms of atherosclerosis of arteries supplying the brain.
WO2006079547A2 Spm 927 for add-on therapy of schizophrenia The present invention is directed to the use of a class of peptide compounds for the prevention, alleviation or/and treatment of a disease that is treated with antipsychotics, in particular psychosis, more particular schizophrenia, in an add-on therapy to at least one antipsychotic.
CN101007831A Nucleic acid molecule RTN4BSR1and its application in preparing anticancer medicine The invention belongs to the field of biological pharmacology, and relates to the use of RTN4BSR1 in preparing antitumor medicament, wherein a nucleotide molecule RTN4BSR1 is provided which can be used for preparing antitumor medicaments, the sequence of the molecule includes 5'-GUGGUUGUUGACCUCCUGU-3', 5'-GTGGTTGTTGACCTCCTGT-3', 5'-ACAGGAGGTCAACAACCAC-3' or 3'-ACAGGAGGUCAACAACCAC-5'. Compared with nude mice containing no RTN4BSR1, the tumor growth of the nude mice containing RTN4BSR1 is inhibited appreciably, which is becoming more appreciable with lapses of time. The invention provides a novel approach for the treatment and alleviation of tumor.
US20050137192 Use of compounds such as 4-bromo-9a-butyl-8-chloro-6-fluoro-7-hydroxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one to treat depression The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
WO2005029980A1 Composition with relieved unpleasant odor or taste of cysteines To provide a composition having a relieved unpleasant odor or taste characteristic to cysteines and a method of relieving the unpleasant odor or taste characteristic to cysteines. A composition having a relieved unpleasant odor or taste characteristic to cysteines which contains cysteines together with a substance swelling in water; and a method of relieving the unpleasant odor or taste characteristic to cysteines characterized by comprising combining cysteines with a substance swelling in water. The relieving effect can be further improved by adding an acidifier or a sweetener.
WO2007144127A1 Pyrrole derivatives with crth2 receptor modulator activity There are provided according to the invention compounds of formula (I) in free or salt form, wherein R3, R 4, R5, R6a, R6b, Q and W are as described in the specification, process for preparing them, and their use as pharmaceuticals.
US6987175 Slurrying in aqueous solution; antibiotics The present invention relates to processes for converting clarithromycin Form I to clarithromycin Form II, which include slurrying clarithromycin the Form I in water. The present invention also relates to processes for the preparation of clarithromycin Form II by converting erythromycin A to clarithromycin and thereafter converting clarithromycin Form I to clarithromycin Form II by slurrying.
US20120165321 Quinoline derivatives as pi3 kinase inhibitors Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
CA2794565A1 Substituted androst-4-ene diones The disclosure relates to novel C4 and C6 substituted androst-4-ene diones as well as andros-1,4-diene diones and derivatives thereof, their process of preparation, pharmaceutical compounds containing them, and the use of said compounds for the treatment of hormone-related disorders in mammals. This includes hormone-dependent cancers, particularly those caused by elevated levels of estrogen and its intermediates. These compounds can also be used in the treatment of other hormone-related disorders, inluding benign prostatic hyperplasia, cardiovascular disease, and neurodegenerative disorders.
CN1590378A Quinoxaline derivative and its preparation method and use A series of quinoxaline derivatives with high immunosuppression activity can be used for organ transplantation and preventing and treating immunopathy, such as nephrotic syndrome, aplastic anemia, rheumatoid arthritis, AIDS, diabetes, SARS, etc. Its preparing process is also disclosed.
US20110207808 Long-chain carboxychromanols and analogs for use as anti-inflammatory agents Provided are long-chain carboxychromanol compounds useful for treating conditions associated with the need to inhibit cyclooxygenase-1, cyclooxygenase-2, and/or 5-lipoxygenase, and pharmaceutical formulations containing the compounds.
US6838547 Acryloyl derivatives of distamycin conjugated with glutathione; have antitumor activity and are thus useful in therapy in the treatment of cancer The present invention refers to distamycin and derivatives thereof, such as bromo- or chloro-acryloyl derivatives of distamycin, which are conjugated with glutathione, to a process for their preparation and to pharmaceutical compositions thereof. The compounds of the invention are endowed with a remarkable antitumor activity and are thus useful in therapy in the treatment of cancer.
CN101016294A Substituted indole-3-oxalamide derivative with multiple bioactivity The invention discloses a substituted indole 3-oxamide derivant and application to treat tumour, prevent virus and inflammatory action, which also provides physiologically acceptable inorganic acid or organic acid salt and their possible N-oxide and excipient and/or diluent, wherein the agent pattern is composed of pill, capsule, dressing tablet, injecting solution or ampoule, bougie, intake powder, suspension agent, emulsion and ointment.
CN102125610A Xiaojin sustained-release pellets and composition thereof The invention discloses xiaojin sustained-release pellets and a composition thereof, belonging to the technical field of medicaments. The xiaojin sustained-release pellets comprise 42-50 percent by weight of medicament-containing fine powder, 50-58 percent by weight of medicinal auxiliary materials and a sustained-release coating layer, wherein the medicament-containing fine powder comprises an adsorbent; the medicinal auxiliary materials comprise filler, a framework material and an adhesive; the sustained-release coating layer comprises the following components in percentage by weight:12-33 percent of plasticizer, 4-17 percent of pore-forming agent, 50-84 percent of sustained-release coating material and 5-20 percent of coating weighting agent. The xiaojin sustained-release pellets can also form a composition with quick-release pellets. Through the xiaojin sustained-release pellets, the medicaments can be effectively controlled to release in 10 hours without a burst release phenomenon. The xiaojin sustained-release pellets and the composition have simple process routes and are easy to realize.
CN103239396A Sodium ibandronate injection composition and preparation method of sodium ibandronate injection composition The invention provides a sodium ibandronate injection composition. Every 1000 injections consist of the following components: 1.0684-6.4101g of sodium ibandronate, 1.66-9.96g of sodium acetate, suitable amount of glacial acetic acid, and 1000-6000ml of water for injection. The sodium ibandronate injection prepared by the invention has the advantages that the prescription is simple, auxiliary materials are all commonly used by the injection, and the safety is high. Simultaneously the sodium acetate content is low, irritation cannot be produced in intravenous administration, the prepared final product is stable in quality, and the indexes of related substances and contents are all superior to those in the prior art.
WO2011080266A1 New secondary 8-hydroxyquinoline-7-carboxamide derivatives. The present invention provides new secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopuiariopsis Brevicaulis. Many of these compounds are active against Candida species such as Candida Albicans and Candida Glabrata.
US20110237550 5-azaindole bisphosphonates Novel 5-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
EP2305283A1 Pharmaceutical compositions for treating dysregulated inflammatory diseases In general, the present invention relates to a new use of lipopeptides or lipoprotein molecules, namely, for treating dysregulated inflammatory diseases. In particular, the present invention relates to pharmaceutical compositions for use in treating dysregulated inflammatory diseases including SIRS, MODS and sepsis. For example, the MALP-2 molecule allows to treat sepsis.
CN103230367A Cefpodoxime proxetil composition dry suspension and preparation method thereof The invention relates to the technical field of medicines and in particular relates to a cefpodoxime proxetil composition dry suspension and a preparation method thereof. The cefpodoxime proxetil composition dry suspension comprises the following materials: cefpodoxime proxetil, sucrose, mannitol and starch slurry. Through the combined action of sucrose, mannitol and starch slurry, the cefpodoxime proxetil composition dry suspension, which is high in dissolution rate, stronger in antibacterial action and good in stability, is obtained on the condition that the process of adding suspending aid is omitted. Moreover, the prepared cefpodoxime proxetil composition dry suspension can be used for preventing medicines from packing and further can be used for strengthening the antibacterial action of the cefpodoxime proxetil.
US20090099094 Use of Somatostatin Agonists to Treat Medullary Thyroid Carcinoma The present invention is directed to a method of determining a treatment to effectively combat medullary thyroid carcinoma and to suppress the secretion of calcitonin from medullary thyroid carcinoma cells. The present invention also provides a method of suppressing the secretion of calcitonin from medullary thyroid carcinoma cells and decreasing the rate of proliferation of medullary thyroid carcinoma cells which comprises contacting medullary thyroid carcinoma cells with one or more somatostatin agonists.
WO2014027826A1 Butenolide-based compound, preparation method therefor, and pharmaceutical composition containing same The present invention relates to: a butenolide-based compound; a stereoisomer thereof; an enantiomer thereof; an in vivo hydrolyzable precursor thereof or a pharmaceutically acceptable salt thereof; and the antibacterial activity, immune disease treatment; and prevention efficacy, the cancer prevention or treatment efficacy, and the preventive activity with respect to the fouling of a medical insertion instrument thereof.
WO2008096746A1 Spiro compound and use thereof Disclosed is a novel SCD inhibitor. Specifically disclosed is a SCD inhibitor comprising a compound represented by the formula (I), a salt thereof, or a prodrug of the compound or the salt. (I) wherein R represents a cyclic group which may be substituted or a carbamoyl group which may be substituted (provided that R is not a 7-pyrido[2,3-d]pyrimidyl group which may be substituted); the ring A represents a pyridazine ring which may be further substituted; R1, R2, R3, R4, R11, R12, R13 and R14 independently represent a hydrogen atom or a substituent, or R1 and R11, R2 and R12, R3 and R13 or R4 and R14 may together form an oxo group, or R2 and R4 may together form a bond or an alkylene crosslink; m and n independently represent an integer of 0 to 2; and the ring B represents a ring which may be substituted (provided that both of the two constituent atoms adjacent to the spiro carbon atom in the ring B are not oxygen atoms).
US8008266 Nucleic acids containing unmethylated cytosine-guanine dinucleotides activate lymphocytes and redirect an immune response from th2 to th1 Nucleic acid sequences containing unmethylated CpG dinucleotides that modulate an immune response including stimulating a Th1 pattern of immune activation, cytokine production, NK lytic activity, and B cell proliferation are disclosed. The sequences are also useful as a synthetic adjuvant.
CN1861587A Internal ester monomer compound and application in preparing anti cancer medicine An anticancer annona lactone monomer 'itrabin' for preventing and treating liver cancer is prepared from the annona seeds through drying, breaking, immersing in petroether, recovering petroether to obtain red oily liquid, laying aside, filtering to obtain white deposit, chromatography, and eluting.
CN1935145A Pharmaceutical use of sophora alkaloids tanate for preventing and treating skin and mucosa infection The present invention relates to an application of tannic acid and its matrine or their composition in preparationof medicine for preventing and curing mucocutaneous infection, including human papillomavirus infection, pointed condyloma, vaginitis, cervicitis and cervical erosion.
EP2361921A2 Novel bicyclonucleoside and oligonnucleotide analogue An oligo- or polynucleotide analogue having one or more structures of the general formula where B is a pyrimidine or purine nucleic acid base, or an analogue thereof, is disclosed. The use of this analogue provides an oligonucleotide analogue antisense molecule, which is minimally hydrolyzable with an enzyme in vivo, has a high sense strand binding ability, and is easily synthesized.
US20060122229 4,5-diarylthiazole derivatives as cb-1 ligands The present invention relates to compounds of formula (I): in which R1 and R2 independently represent phenyl, thienyl or pyridyl and R3 represents a group —X—Y—NR4R5 in which X is CO or SO2; Y is absent or represents NH and the other substituente are as defined in the description and their use in the treatment of obesity, psychiatric and neurological disorders and to pharmaceutical compositions containing them.
US20110082101 Combinations comprising epothilones and anti-metabolites Disclosed is a combination which comprises (a) an antineoplastic antimetabolite and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl, R′ is methyl, methoxy, ethoxy, amino, methylamino, dimethylamino, aminomethyl or methylthio, and Z is O or a bond, and optionally at least one pharmaceutically acceptable carrier and/or, optionally, a standard anti-diarrheal, for simultaneous, separate or sequential use, in particular for the treatment of a proliferative disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal.
US20080312293 2-Arylpropionic Acid Derivatives and Pharmaceutical Compositions Containing Them The present invention relates to selected (R)-2-phenyl-propionamides and (R)-2-phenyl-sulfonamides with a hydrogen bond acceptor atom/group in a well defined position in the chemical space. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
WO2008096119A1 Salts 669 A pharmaceutically acceptable salt of N-[2-(Diethylamino)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(3-chlorophenyl)ethoxy]pro panamide provided it is not the ditrifluoroacetate salt; and the use of such a compound as a medicament (for example in the treatment of respiratory diseases (such as asthma or COPD).
US7420050 TGF-β-specific covalently closed antisense molecule The present application describes a purified covalently closed antisense molecule, which specifically inhibits expression of TGF-β.
EP1550443A1 Composition against stress-related diseases It is intended to provide an improved drug, compared with the existing ones, for stress-related diseases which comprises a combination of lysine wi than agent for stress-related diseases other than lysine, in particular, a drug for stress-related diseases having an enhanced effect (drug efficacy) and reduced side effects. The above drug, which can be employed in the form of a medicine (including a medicine for animals), a food, a drink or a feed, is highly useful in preventing, treating or ameliorating various stress-related diseases and preventing the progress of such diseases. The two ingredients as described above can be used either at the same time or at different points in different forms. It is also intended to provide a method of preventing and treating stress-related diseases, utilization of the above active ingredients in a preventive/remedy for stress-related diseases and so on.
EP1129077B1 Fluorinated 3,4-dihydroquinoline derivatives used as nos inhibitors The invention relates to compounds of formula (I), to a method for producing them and to their use in medicaments as NOS inhibitors.
CN101259139A Pharmaceutical composition for anti-inflammation ease-pain The invention provides an anti-inflammatory and pain-killing medical composition; chondroitin sulfate and a non-steroidal anti-inflammatory agent are used as active ingredients and mixed with a medical carrier to form the composition. Non-steroidal anti-inflammatory agent includes but not confines in diclofenac sodium (potassium), naprosyn and Lornoxicam; the composition exists in forms of squirt, freeze-dried powder and large-capacity transfusion for intravenous medication of a human body. The composition can be applied to symptomatic treatments of various febrile illnesses, various arthritises and inflammatory rheumatic diseases, soft tissue rheumatisms, neuralgia, arthralgia and pains, wounds relevant to degenerative diseases of spines, or postoperative pains.
CN102920655A Florfenicol suspension injection and preparation procedure thereof The invention discloses a florfenicol suspension injection and a preparation procedure thereof, and relates to a medicine and a preparation procedure. The drug substance of the florfenicol suspension injection provided by the invention comprises the following components in part by weight: 40-100 parts of fat soluble florfenicol, 1.5-5 parts of suspending agent, 2-4 parts of wetting agent, 0.8-1.2 parts of citric acid, 0.3-0.5 parts of sodium citrate, 0.5-1 part of butylated hydroxytoluene and 5-40 parts of benzyl alcohol. The preparation procedure comprises the following steps: water for injection is used to dissolve the prescribed suspending agent into rubber paste to get solution 1; fat soluble florfenicol is evenly mixed with a wetting agent and water is added into the mixture of the fat soluble florfenicol and the wetting agent to form suspension to get solution 2; solution 1 is slowly added to solution 2 while stirring; citric acid, sodium citrate, butylated hydroxytoluene and benzyl alcohol is added, and then water is added to get 1000 ml of suspension; and the suspension is split and packed after stirring for 30-40 minutes to get florfenicol suspension injection. The florfenicol suspension injection has the advantages of broad antibacterial effect, strong antibacterial activity, low dosing frequency, little stress response and low price.
WO2014011902A1 Irak inhibitors and uses thereof The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.
CN103356759A Medicament for treating climacteric syndrome, and preparation method thereof The invention discloses a medicament for treating climacteric syndrome, and a preparation method thereof. The medicament is mainly prepared from polygonum multiflorum, monkshood, cinnamon, red ginseng, bezoar, ligusticum wallichii, angelica sinensis, progesterone and the like by a certain weight ratio. The medicament disclosed by the invention has the functions of strengthening spleen, tonifying kidney, reinforcing qi, nourishing blood, nourishing Yin, moistening dryness, invigorating kidney and securing essence, and becomes effective quickly, realizes good treatment effect and has a high cure rate when being used for treating climacteric syndrome.
EP1098986B1 A polynucleotide comprising a ubiquitous chromatin opening element (ucoe) The present invention relates to a polynucleotide comprising a ubiquitous chromatin opening element (UCOE) which is not derived from an LCR. The present invention also relates to a vector comprising the polynucleotide sequence, a host cell comprising the vector, use of the polynucleotide, vector or host cell in therapy and in an assay, and a method of identifying UCOEs. The UCOE opens chromatin or maintains chromatin in an open state and facilitates reproducible expression of an operably-linked gene in cells of at least two different tissue types.
CN103705552A External liniment with function of improving allergy The invention discloses an external liniment with a function of improving allergy. The external liniment comprises the following components in percentage by mass: 65-74 percent of blackcurrant seed oil, 8-12 percent of gamma-linolenic acid, 8-12 percent of blackcurrant extracting solution, 2-4 percent of anthocyanin, 1-3 percent of vitamin C, 0.5-0.8 percent of zinc-containing compound, 1-3 percent of beeswax, 1-4 percent of lecithin and 0.2-0.5 percent of borneol, wherein the total mass percent of the components is 100 percent. According to the external liniment, decoction consisting of 20-30 parts of fructus forsythiae, 10-18 parts of cynanchum paniculatum, 6-8 parts of mint and 2-4 parts of liquorice is used singly or taken in a matched mode and is used for improving the skin allergy. The gamma-linolenic acid and anthocyanin enriched in the blackcurrant seeds and peels have the effects of promoting blood circulation, regulating the prostaglandin balance of a body and improving the immune system, and the external liniment is prepared by utilizing the residual seeds and fruit residues in the blackcurrant processing process, so that the treatment effect of improving the allergy symptoms is achieved.
CN1562015A Sugar-free stop-smoking lozenge A non-sugar bucal lozenge for giving up smoking and preventing dental caries is prepared from xylitol, nicotin adhesive, essence and magnesium (calcium) stearate.
CN102807568A Thiadiazole derivative DPP-IV (dipeptidyl peptidase IV) inhibitor The invention relates to thiadiazole derivatives which are shown as a formula I and have DPP-IV (dipeptidyl peptidase IV) inhibition activity, a preparation method of the thiadiazole derivatives and drug compositions of the thiadiazole derivatives, and application of the thiadiazole derivatives to treatment of diseases beneficial from DPP-IV inhibition, especially application to treatment of diabetes mellitus type 2. The thiadiazole derivatives provided by the invention have very good DPP-IV inhibition activity, have a very good in-vivo metabolic level and a very proper in-vivo half-life period and are expected to be used as proper DPP-IV inhibitor drugs.
CN101967134A Compound separated and extracted from marine penicillium sp.QY013 and application thereof The invention relates to a compound separated and extracted from marine penicillium sp.QY013 and application thereof. In the method, a monomeric compound which has the chemical name of 5,6 dihydro-4-methyl-2H-pyran-2-ketone and is provided with a quorum sensing system for inhibiting pseudomonas aeruginosa and chromobacterium violaceum is prepared by performing fermentation culture, separation and purification on the strain QY013. The compound has an action mechanism totally different from that of the conventional antibacterial medicament, only inhibits bacterial quorum sensing controlled pathogenic behaviors and does not influence the growth of bacteria, so bacterial medicament resistance cannot be generated theoretically. The compound has the advantages that: raw materials are readily available, the strain is easy to ferment and culture, the preparation process is easy to control, the yield is high, and the like. The compound and derivatives thereof can be developed into novel bacterial medicaments for the fields such as clinical use, agricultural production and the like, and has great significance for human health and agricultural production.
CN101366708A Application of alpha-ararin in preparing anxiolytic and antidepressant medicament The invention belongs to the technical field of medicine and relates to application of alpha-asarin in preparing antianxiety and antidepressant medicines. The invention aims to provide the application of the alpha-asarin in preparing the antianxiety and antidepressant medicines. The alpha-asarin can constitute medical compositions with various pharmaceutical carriers or constitute compound medicines with other medical components; the alpha-asarin and the medicine compositions and the compound medicines of the alpha-asarin can be taken by oral, parenteral or local means; and the delivery dosage form can be pharmaceutically acceptable dosage forms such as tablets, capsules, solution, suspension, injecta and so on. The alpha-asarin has novel application of antianxiety and anti-depression, has small toxicity, has no defects of general antianxiety and antidepressant medicines such as calmness, ataxia, activated epilepsy and so on, and has good development and application prospect.
CN102327276A Injecta for treating bacterial encephalitis of dog and preparation method thereof The invention discloses injecta for treating bacterial encephalitis of a dog and a preparation method thereof, and aims at providing the injecta for treating bacterial encephalitis of the dog effectively and efficiently, with an effect for treating both principal and secondary aspect of the disease as well as the preparation method with a simple process and easiness in realization. Every 100L of injecta comprises 5-15kg of sulfadiazine sodium, 10-20kg of analgin, 1-3kg of trimethoprim, 0.1-0.2kg of chlorphenamine, 10kg of dimethylformamide, 10kg of 95 percent ethanol, 30kg of propanediol and the balance of water for injection. The sulfadiazine sodium adopted by the invention has a wide spectrum antimicrobial function and can be used for transmitting through a blood brain barrier and killing bacteria; the trimethoprim is a synergistic agent and can be used for enhancing the antimicrobial effect of the sulfadiazine sodium and changing the traditional bacteriostatic action into bactericidal action; the analgin has functions of defervescing and resisting inflammation and can be used for reducing the damage to an immunologic system and nerve of the dog caused by high fever; and the chlorphenamine has the functions of resisting hypersusceptibility and calming and can be used for reducing an anaphylactic reaction caused by toxin generated by bacteria.
EP1623705A1 Use of phenylethanolaminotetralines for preparing anxiolytic drugs Use of at least one phenylethanolaminotetraline of general formula (I): wherein A represents a (C1-C4)alkylene group, and R is hydrogen or a (C1-C4)alkyl group, or one of its pharmaceutically acceptable salts, for the preparation of a drug for treating anxiety disorders.
CN103564089A Medicinal tea bag The invention relates to a medicinal tea bag, wherein on the basis that Chinese tea culture theories are combined with modern nutrition theories, the core idea of the medicinal tea bag is to internally recuperate, whiten, remove freckle and beautify; angelica sinensis, carthamus tinctorius, white poria, lily and the like are compatible; and the medicinal tea bag disclosed by the invention has the effects of moistening and nourishing the viscera, nourishing blood, adjusting vitality, dredging the channel, tonifying spleen, dehumidifying and the like.
WO2006108482A1 Purine derivatives as receptor-tyrosine kinase activityinhibitors The invention relates to compounds of formula (I), whereon R1, R2, R3, R4 and X have the meanings cited in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and the Raf-kinases and can be also be used for treating tumours.
CN102389245A Formula of health care medicine pillow for detoxifying and health-promoting The invention relates to a medicine pillow, in particular to a formula of a health care medicine pillow for detoxifying and health-promoting. The medicine pillow consists of pine needles, gingko leaves, mulberry leaves, tomato leaves, loquat leaves, mugwort leaves, Apocynum venetum L. leaves, Platycodon grandiflorum, mint, folium perillae, tomato twigs, mulberry twigs, cassia twigs, white chrysanthemum, flos Albizzia, Ligusticum wallichii, siberian ginseng, caulis polygoni multiflori, selfheal, liquorice, garden balsam stem, Lycopodii herb, black tea, Cassia obtusifolia L., silkworm excrement, magnetitum, negative ion ceramic particles and far-infrared ceramic particles. The medicine pillow has the functions of tranquilizing the mind, purifying blood, stabilizing blood pressure, stabilizing blood sugar, regulating Qi and relieving asthma and regulating the immune function of human body. The medicine pillow has simple preparation method and low cost and is convenient to use, and is easy to post.
CN103550252A Preparation method of Fe slow-release preparation as well as prepared slow-release preparation The invention relates to the field of preparation of slow-release preparations, and particularly relates to a preparation method of a Fe slow-release preparation and the Fe slow-release preparation prepared according to the method. The preparation method of the Fe slow-release preparation comprises the following steps: adding a quaternary ammonium salt type cationic surface active agent into a mixed system of ethanol and water; adding an assistant template, ammonium water and tetraethoxysilane into the system to obtain a colloidal mixed system; hermetically placing the colloidal mixed system for 2-5 days at room temperature, filtering to obtain a precursor of a silicon-based mesoporous molecular sieve, and washing, drying and roasting the precursor of the silicon-based mesoporous molecular sieve to obtain the silicon-based mesoporous molecular sieve; and adding the silicon-based mesoporous molecular sieve into supersaturated solution containing divalent Fe ions, and carrying out ultrasonic treatment to obtain the Fe slow-release preparation. The ultrasonic-assisted dispersion technology is adopted and the efficiency and effect of dispersing Fe ion to solid phase are improved. The Fe-loading amount of the Fe slow-release preparation prepared by the method is about 10% and the release rate of Fe is slow.
US20140030325 Long-acting and controlled release formulations of 2-[(3-chlorophenyl) amino] phenylacetic acid Formulation of long-acting and controlled release preparations of 2-[(3-chlorophenyl)amino] phenylacetic acid (23CPPA) are disclosed. Long-acting preparations comprise a slow-release formulation coated onto a pharmaceutical composition containing 23CPPA, protect against gastric irritation, slow absorption of 23CPPA, extend release of 23CPPA, protect against excessively high 23CPPA blood concentrations, and prolong maintenance of blood concentrations of 23CPPA after administration. Controlled release formulations comprise (a) a core element which is a compressed tablet containing a therapeutic dose of 23CPPA and an amount of a solubility modulating substance that controls the release of said 23CPPA in order to provide a therapeutic level over a period of about 24 hours; and (b) on the outer surface of the core element, a sufficient amount of an enteric coating that causes the 23CPPA to release at a rate that permits the use of once-a-day dosing to maintain steady state therapeutic levels of 23CPPA.
CN1951445A Itching relieving lotion and preparation method thereof The invention discloses a lotion against itching, wherein each 1000ml of the lotion comprises flavescent sophora root 50-70g, yellow corktree bark 50-70g, Chinese prickly ash 15-25g, borneol 0.5-2g, cnidium fruit 25-35g, dittany bark 25-35g, menthol 0.5-2g, domiphen bromide 0.5-2g. The preparing process of the lotion comprises steps of immersing cnidium fruit and pricklyash peel with 20 times by weight of water, distilling and collecting volatile oil, charging 5ml of Tween-80, grinding into slag, gathering distilled aqueous solution, merging raw materials and charging 12 times by weight of water for immersion, grilling and filtering, charging 10 times by weight of water into drug dross, grilling twice, filtering the decoction liquid, merging the filter liquor, filtering and merging the filter liquor with distilled aqueous solution, obtaining extract through decompression and concentration, charging ethanol to content of 60%, homogenizing, stewing, extracting supernatant fluid, reclaiming ethanol till no alcohol smell is present, and diluting to 1000ml with water.
CN103272208A Agent for curing myeloma The invention relates to an agent for curing myeloma. The agent contains the following materials in ratio by weight: 100-150 parts of berchemia lineate, 10-15 parts of glabrous sarcandra herb, 10-15 parts of ardisia crenata, 20-30 parts of root of rehmannia, 25-30 parts of cudrania cochinchinensis kudo et masam, 30-35 parts of radix zanthoxyli, 12-15 parts of buddleja lindleyana, 7-15 parts of honeysuckle, 10-15 parts of forsythia suspense, 7-10 parts of ternate grape fern herb, 10-15 parts of platycodon grandiflorus, 15-17 parts of radix isatidis, 40-50 parts of gypsum, 15-20 parts of cirsium japonicum, 12-15 parts of radix angelicae, 15-21 parts of lalang grass rhizome. 15-20 parts of polygonum cuspidatum, 12-15 parts of rhodiola rosea, 15-25 parts of radix salviae miltiorrhizae, 7-12 parts of common sage herb, 70-100 parts of red date, 5-7 parts of liquorice, 5-7 parts of cassia twig and 30-50 parts of rhizoma zingiberis. The agent for curing myeloma has the characteristics of low cost, easy preparation, small toxic and side effects and significant effect.
WO2011093470A1 Pharmaceutical composition for treatment of bone diseases, which contains protein comprising bone morphogenetic protein receptor 1b (bmpr1b) extracellular domain or mutant thereof Disclosed is a pharmaceutical composition for the treatment of bone diseases, which contains, as an active ingredient: a protein that comprises a bone morphogenetic protein receptor 1B (BMPR1B) extracellular domain derived from a mammal or a mutant of the BMPR1B extracellular domain, said mutant having 85% or higher sequence identity with the amino acid sequence of the domain and having an effect of increasing the bone mass, bone density and/or bone strength; or a vector comprising a nucleic acid encoding the protein. Examples of the bone diseases may include osteoporosis, osteoarthritis, rheumatoid arthritis, bone diseases associated with malignant tumors or the like, and various bone diseases or disorders associated with the aforementioned diseases.
US7767850 S-[2-[(1-iminoethy)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride crystalline salt A novel mixed salt of S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine is disclosed. The novel mixed salt, S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, may be produced to form crystals that may be arranged as generally orderly packed agglomerates, which are particularly useful in making pharmaceutical compositions. Such pharmaceutical compositions are also described, as well as methods to make crystalline S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, and methods of treating conditions characterized by an overexpression on nitric oxide from the inducible isoform of nitric oxide synthase using the S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride.
US20100150986 Film preparation with rapidly dissolving property and flexibility The present invention relates to a film preparation having both rapid solubility and flexibility at the same time. The film preparation is characterized by comprising: an active-ingredient-containing layer comprising an active ingredient, a water-soluble polymer selected from the group consisting of methyl cellulose, hydroxypropyl cellulose, and hydroxypropyl methyl cellulose, and a disintegrating agent; and an active-ingredient-free layer comprising methyl cellulose and/or hydroxypropyl methyl cellulose. It is further characterized in that the amount of the active ingredient is 0.1-75.0 mass % of a total mass of the film preparation and a total content of the active ingredient and the water-soluble polymer in the active-ingredient-containing layer is 15.0-95.0 mass % of a total mass of the active-ingredient-containing layer.
CA2384037C Pyrazolo[4,3-d]pyrimidines Pyrazolo[4,3-d]pyrimidines of the formula I (see formula I) and their physiologically acceptable salts, in which R1, R2, R3, R4 and X have the meanings indicated in Claim 1, exhibit phosphodiesterase V inhibition and can be employed for the treatment of disorders of the cardiovascular system and for the treatment and/or therapy of potency disorders.
WO2009114718A2 Methods and assays for detecting and treating hypoglycemia Methods for regulating glucagon release and of treating hypoglycemia, and for screening drug candidates for treating hypoglycemia. The methods are useful for treating diabetes mellitus and screening drug candidates for potential efficacy.
WO2011148956A1 Fused imidazole derivative Provided is a novel compound which has antagonistic activity against a T-type calcium channel and is useful as a medicine. The compound is represented by general formula (I) (wherein n, indicating the number of nitrogen atoms contained in the fused 6-membered aromatic ring, is 0, 1, or 2; p, indicating the number of nitrogen atoms contained in the 6-membered aromatic ring, is 0 or 1; X represents an oxygen atom, -SO2-, or -N(R9)-; and R1 to R5 each represents a hydrogen atom or a substituent). Also provided is a medicine containing the compound.
WO2005000203A2 Methods for treating cognitive impairment and improving cognition Cognitive impairments are treated and cognition is improved with an amphetamine compound. In one embodiment, the method includes administering an I-amphetamine compound. In another embodiment, the method includes administering an 1-methamphetamine compound.
US20120196896 Treatment for Oxidative Stress and/or Hypertension One aspect of the invention relates to compounds, compositions and methods for treating oxidative stress and/or hypertension. In certain embodiments, the invention relates to a mixture of tempol and an angiotensin receptor blocker (ARB) and the use of said mixture to treat oxidative stress and/or hypertension. In certain embodiments, the invention relates to a tempol/ARB adduct and the use of said adduct to treat oxidative stress and/or hypertension.
CA2336712C Transdermal plaster containing at least one active ingredient which influences blood serum lipid levels A preparation containing at least one active substance having an influence on the lipid blood levels of an organism is characterized in that it is present in the form of a transdermal therapeutic patch containing the active substance in a self-adhesive matrix layer which can be covered at the side facing away from the skin with an active substance--impermeable backing layer
CN102188421A Fluvastatin preparation without stabilizing agents The invention provides a fluvastatin preparation without stabilizing agents. The fluvastatin preparation is characterized in that the fluvastatin preparation does not contain alkalizers for elevating the pH value of the preparation; fluvastatin is dispersed on pharmaceutically applicable polymer carriers to achieve the aim of stabilization; and the polymer carriers are selected from one or more of polyethylene glycols, polyvidones, surfactants containing polyoxyethylene groups, water-soluble cellulose derivatives, organic acids, saccharides and alcohols. The preparation can be prepared by a freeze drying method.
CN103720709A Cell apoptosis inducer containing chlorine dioxide and application thereof to preparation of cosmetics, or anti-aging or antineoplastic drugs The invention relates to a cell apoptosis inducer containing chlorine dioxide, and further relates to a cell apoptosis inducer kit which comprises two independent components: a first component: chlorine dioxide precursor solid, or a solution containing a chlorine dioxide precursor; a second component: a water solution of an acidity pH adjuster; the two components are stored independently, and can be mixed before use to react with each other on site, so as to prepare the cell apoptosis inducer containing chlorine dioxide; moreover, the amount and concentration of the first component and the second component enable the pH of the mixed solution to be 1.5-6.5. The invention further relates to application of the cell apoptosis inducer containing chlorine dioxide or the cell apoptosis inducer kit containing chlorine dioxide to the preparation of drugs for treating tumors or anti-aging drugs for target tissues of mammals or chemotherapeutic drugs, or being used as cosmetics.
US20110177035 Use of secretor, lewis and sialyl antigen levels in clinical samples as predictors of risk for disease An individual at risk for necrotizing enterocolitis and related disorders can be identified by measuring the level of at least one secretor antigen in a biological sample from the individual and comparing the measured level of the at least one secretor antigen to a predetermined value or a predetermined range of values. Among the secretor antigens which can be measured are: the H-1, H-2, Lewisb and Lewisy antigens and derivatives thereof (e.g., a sialylated form of Lewis a, Lewis x, Lewis b, Lewis y; H-1, H-2, Lewis a, Lewis x, Lewis b or Lewis y).
EP1474109B1 Use of synthetic inorganic nanoparticles as carriers for ophthalmic drugs The use of nanoparticles of inorganic materials (e.g., synthetic smectite clays) in ophthalmic and otic pharmaceutical compositions is described. The nanoparticles are utilized as biologically inert carriers or depots for ophthalmic and otic drugs. The nanoparticles may also be utilized to modify the rheological properties of the compositions, so as to enhance the viscosity or flow characteristics of the compositions and/or increase the retention time of the compositions in the eye or ear.
US20110237583 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer The present invention relates to pyridopyrimidine derivatives according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
US7879817 Non-steroidal anti-inflammatory drugs bound to hyaluronic acid through a covalent bond via a spacer having a biodegradable region and disease-modifying anti-rheumatic drugs; salicylic acid, aspirin, mefenamic acid, tolfenamic acid; arthritis, suppress inflammation and pain; parenteral, topical A hyaluronic acid derivative in which an anti-inflammatory drug is bound to hyaluronic acid through a covalent bond via a spacer having a biodegradable region, and a production process thereof.
CN103463025A Application of Lycojaponicumin B in medicine for treating lung cancer The invention discloses an application of Lycojaponicumin B in preparation of a medicine for treating lung cancer. The compound, namely the Lycojaponicumin B shows high lung cancer resisting activity, can be used for preparing a lung cancer resisting medicine and belongs to the technical field of new applications of medicines. The Lycojaponicumin B can obviously inhibit the non-small-cell lung cancer cell A549, maxicell lung cancer cell NCI-H460, squamous cell lung cancer cell HTB-8 and human lung squamous epithelium cancer cell QG-5 cultured in vitro while realizing a relatively low effect on inhibiting the human normal liver cell LO2 and the peripheral blood lymphocyte cell, thereby showing obvious selectivity. The application of the Lycojaponicumin B in preparation of the medicine for treating lung cancer is disclosed for the first time; the skeleton type of the Lycojaponicumin B belongs to a brand new skeleton type, and the inhibitory activity of the Lycojaponicumin B on lung cancer cells is unexpectedly strong.
US20110064660 Deuterated alkyl phospholipid compounds, compositions, and methods of use The invention generally relates to novel deuterated phospholipid compounds, compositions comprising these compounds, and their use in a variety of cancer therapy and diagnostic applications.
US7250453 Polyolefins with bactericide for molding materials, polyesters, polyamides or olefin polymers formed into moldings with fines for composites. Anti-bacterial composite particles which comprise a polymer base material comprising a thermal melting polymer, such as a polyolefine, exhibiting good dispersibility in a basic material resin and having a lower molecular weight or a lower softening point than that of the basic material resin, and inorganic fine particles comprising a metal having anti-bacterial activity carried thereon. An antibacterial resin composition can be prepared by melting and kneading a synthetic resin composition as the basic material resin together with the anti-bacterial composite particles and forming by known molding methods such as extrusion molding and injection molding, and can be used for producing various synthetic resin moldings which have an inorganic anti-bacterial agent uniformly dispersed in a synthetic resin composition and thus exhibits good anti-bacterial effect.
US7064138 Also treating bulimia nervosa, irritable bowel syndrome, urinary incontinence, asthma, bradycardia, and bradyarrhythmia Methods for the prophylaxis, treatment, or management of irritable bowel syndrome using (−) norcisapride, or a pharmaceutically acceptable salt thereof, substantially free of its (+) stereoisomer are disclosed.
WO2008031440A3 Isoniazid mediated healing of wounds and ulcers The invention relates to the use of a compound(s) selected from isoniazid and isoniazid analogs of formula Ia, wherein R is -C(O)NHNH2, -C(O)NHNHC1-6 alkyl, -C(O)NHN=C1-6 alkenyl, -C(O)NHNHC2-6 alkenyl, -C(O)NHC1-6 alkyl, -C(O)NHC2-6 alkenyl, -C(O)NHNHC(O)C1-6alkyl, -NHC(O)C1-6 alkyl, -NHC(O)C1-6 alkenyl, -NHC(O)NH2, -NHC(O)NHC1-6 alkyl, -NHC(O)NHC2-6 alkenyl, or -COOH, and wherein formula (Ia) optionally is further substituted with one or more substituents; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the preparation of a pharmaceutical composition for treating a condition selected from the group consisting of cutaneous lesions, wounds, ulcers and infarcts in a tissue area with compromised vascularisation, in an animal, such as a human subject. The compound is preferably isoniazid, or pharmaceutical acceptable salts, solvates or prodrugs thereof, and the conditions to be treated is for example selected from the group consisting of pressure ulcers, diabetic ulcers, arterial ulcers and anastomotic ulcers. The invention furthermore relates to a method of treating a condition selected from wounds, ulcers or infarcts in a tissue area with compromised vascularisation in an animal, such as a human subject.
EP1490333B1 New atorvastatin salts and pharmaceutical compositions containing them The invention relates to salts of atorvastatin formed with a basic amino acid of the general formula (I), where the meaning of R is a group originated from lysine, arginine or ornithine, and the amorphous or polymorph modifications thereof. The invention also relates to the synthesis of the compounds of the general formula (I).
WO2003087338A3 Her-2 receptor tyrosine kinase molecules and uses thereof The present invention provides HER-2 Receptor Tyrosine Kinase polypeptides and nucleic acid molecules encoding the same. Specifically, the present invention relates to splice variants of HER-2 (HER-2sv). The invention also provides selective binding agents, vectors, host cells, and methods for producing HER-2sv polypeptides. The invention further provides pharmaceutical compositions and methods for the diagnosis, treatment, amelioration, and/or prevention of diseases, disorders, and conditions associated with HER-2sv polypeptides.
CN103735525A Dapoxetine tablets and preparation method thereof The invention relates to dapoxetine tablets and a preparation method thereof. The dapoxetine tablets comprise the following components in percentage by weight: 10 to 50 percent of dapoxetine, 30 to 80 percent of a filling agent, 3 to 20 percent of a disintegrant, 0.5 to 1 percent of a lubricant and 0.2 to 2.5 percent of a flavoring agent. The preparation method comprises the following steps: micronizing the dapoxetine and the filling agent and controlling the particle size to be 0.5-20 [mu]m; preparing the fine powder obtained in the previous step and a part of the disintegrant into a soft material by ethanol water and pelletizing by a 24-mesh sieve; drying the obtained fine particles at the temperature of 50 to 70 DEG C and straightening by a 20-mesh sieve; sequentially adding the rest disintegrant, the flavoring agent and the lubricant into the dried particles, carrying out blending for two times, and until intermediates are qualified by detection, and carrying out tabletting, so that the dapoxetine tablets are obtained, wherein blending is carried out for one time before the lubricant is added and then is carried out again after the lubricant is added. The dapoxetine tablets are coated or uncoated conventional tablets, chewable tablets and orally disintegrating tablets, are used for treating male prospermia, high in drug adsorption speed and bioavailability, and convenient to take and have small side effects.
US20100267772 Combination of a Serotonin Reuptake Inhibitor and Agomelatine The present invention relates to the use of a combination of agomelatine and a serotonin reuptake inhibitor (SRIs), or any other compound, which causes an elevation in the level of extracellular serotonin, for the treatment of depression and other affective disorders.
WO2009063235A1 Derivatives of 1,9-dihydro-6h-purin-6-one and uses thereof-018 The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I): which have bacterial MurI inhibitory activity and are accordingly useful for their treatment and prophylaxis of bacterial infection, e.g., E.faecalis or E. faecium infection. Further, the invention relates to methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of the compounds, to pharmaceutical compositions containing them, and to their use in the manufacture of medicaments of use in the treatment and prevention of various bacterial diseases in a warm-blooded animal such as man.
US20110142905 Coated tablets with remaining degradation surface over the time The present invention relates to a pharmaceutical composition for controlled delivery of at least one active ingredient into an aqueous phase, said pharmaceutical composition comprising: a tablet, preferably obtainable by compression, said tablet comprising said at least one active ingredient and optionally excipients; and a coating, applied on said tablet, said coating covering at least part of said tablet to impede the release of said at least one active ingredient from at least part of the surface of said tablet, said coating being applied in a manner allowing the release of said at least one active ingredient from said tablet after contacting said pharmaceutical composition with said aqueous phase, establishing one or more degradation surfaces of said tablet; wherein the first derivative of the area of each degradation surface with respect to time is larger than or equal to zero.
EP1096934B1 Oxazolidinones to treat eye infections The present invention involves a method of treating an ophthalmic infection in a useful warm blooded mammal who is in need of such treatment which comprises topical administration of an ophthalmologicallly effective amount of an OXAZOLIDINONE.
WO2004041258A8 Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses The invention concerns the use of PDE2 inhibitors for treating disorders of the central and peripheral nervous system, a method for therapeutic treatment by administering to an animal said inhibitors. More specifically, the invention concerns novel benzodiazepinone derivatives and their uses in therapeutics more particularly for treating pathologies involving activity of type 2 cyclic nucleotide phosphodiesterase. The invention also concerns methods for preparing same and novel synthesis intermediates.
CN102973566A DPAs and high-molecular polymer used for hyperlipemia and for reducing fat animal food absorbing amount and fat tissue weight The invention provides DPAs type or/and high-molecular polymer used for improving hyperlipemia, atherosclerosis and for reducing fat animal food absorbing amount and fat tissue content.
EP2247286A2 Alcohol antimicrobial skin sanitizing compositions including cationic compatible thickeners The present disclosure generally relates to alcohol antimicrobial skin sanitizing compositions for use in hand washing and skin sanitizing. The antimicrobial skin sanitizing composition comprises an alcohol for providing effective antimicrobial control, one or more cationic compounds for moisturizing and protecting the skin, and a compatible thickening system for thickening the antimicrobial skin sanitizing composition. The antimicrobial skin sanitizing compositions can be used alone or in combination with personal care products.
CN101747339A 1'-thio-aza indirubin compound, application and preparation method thereof The invention discloses a 1'-thio-aza indirubin compound, application and a preparation method thereof, belonging to the field of medical technology. The preparation method of the compound comprises the steps of: respectively condensing 5-substituted, 6-substituted, 7-substituted isatin derivatives or 1-alkyl-7-azaindole-2,3-dione with thieno-(2,3-b)-pyridine-3-ketone or benzo-3(2H)-ketone to obtain a 1'-thio-aza indirubin compound in which R=O, wherein sodium carbonate is used as a catalyst; and reacting the 1'-thio-aza indirubin compound in which R=O with hydroxylamine to obtain a 1'-thio-aza indirubin compound in which R=NOH. The invention also relates to the application of the compound in the preparation of antineoplastic agents, acceptable salts in pharmacy synthesized by the compound with inorganic acid, organic acid or amino acid. The compound of the invention can suppress or kill tumor cells, have the character of anti-tumor activity and can be used for preparing medicines for treating tumors.
US20090253668 such as N-[(2,4-Dihydroxyphenyl)ethylidene]cysteine zinc salt for topical application; antiaging agents, antigreying agents This invention relates to certain skin and hair care agents of formula (I), derived from natural amino acids and peptides. These agents provide multi-functional treatment of enzyme-related skin, hair and scalp problems, for example, hair aging including premature hair loss and hair graying; male pattern baldness; hair loss from dandruff; alopecia; split ends, acne, darkened skin, dark circles around eyes, stretch marks, wrinkles and fine lines, loss of collagen, loss of skin pliability and combinations thereof:
CN102058526A Nicardipine hydrochloride fructose injection and preparation method thereof The invention provides a nicardipine hydrochloride fructose injection which comprises 0.01-0.1% (g/mL) nicardipine hydrochloride and 5-10% (g/mL) fructose, wherein the pH value is 4.5+/-0.1. The invention also provides a preparation method of the nicardipine hydrochloride fructose injection. The injection prepared by the invention is used for patients suffering from hypertension with diabetes mellitus and perioperative hypertension, can be used for quickly, safety and stably controlling blood pressure, has a good curative effect and less side effect and is convenient to store; and meanwhile, the preparation process is simple and is favorable for popularization and application.
US20100015249 Antitumor agent containing 6'-amidino-2'-naphthyl 4-guanidinobenzoate or salt thereof It is an object of the present invention to provide novel antitumor agents which have a high therapeutic index while causing neither serious adverse effects nor drug resistance, both of which are the problems associated with existing antitumor agents. In particular, it is an object of the present invention to provide novel agents and therapies which are effective for pancreas cancer, for which no effective therapies and chemotherapeutic agents exist at this stage, and are also capable of inhibiting cancer metastasis and cancer filtration. The antitumor agents, more specifically the therapeutic agents for pancreas cancer and the cancer metastasis inhibitors, of the present invention contain as an active ingredient 6′-amidino-2′-naphthyl 4-guanidinobenzoate or a salt thereof or more specifically the mesylate thereof known as nafamostat mesilate (generic name; also referred to as “Futhan,” “FUT,” and “FUT175.”). Moreover, in another mode of the present invention, the above mentioned FUT is administered in combination with existing anticancer/antitumor agents, particularly preferably in combination with gemcitabine hydrochloride.
US20120165281 Stilbenoid derivatives and their uses The present invention generally provides stilbenoid derivatives and methods for using stilbenoid derivatives to modulate the activity of cannabinoid receptors or scavenge reactive nitrogen species.
US20120289593 Methods for risk assessment, treating, and diagnosing myocardial infarction This document features method related to genetic markers associated with myocardial infarction. For example, methods of using such genetic markers for risk assessment and for diagnosing and treating myocardial infarction are provided.
US20120283302 Scca-1 production inhibitor having a carboxamide derivative and/or a salt thereof as an active ingredient A SCCA-1 production inhibitor, comprising as an active ingredient, at least one carboxamide derivative selected from the group consisting of compounds represented by the following formula (I): wherein X is CR5 or N, R1, R4 and R5 each independently represent hydrogen, C1-C4 alkyl or a C1-C6 hydroxyalkyl group having 1-5 hydroxy groups, R2 and R3 each independently represent hydrogen, C1-C4 alkyl or a C1-C6 hydroxyalkyl group having 1-5 hydroxy groups, or each represents a group —(CH2)n—, wherein n represents an integer of 1 or 2, and may form a 5- to 6-membered ring together with the atoms to which they are bonded and with the carbonyl group, allantoin, and salts thereof.
CN103006693A Double-vitamin calcium carbonate composition The invention relates to a double-vitamin calcium carbonate composition belonging to the technical field of medicine. The composition comprises the following active components: 300-3500 parts by weight of calcium carbonate, 0.1-60 parts by weight of vitamin K and 0.001-0.1 part by weight of vitamin D. According to the invention, because of the scientific formula, calcium can be effectively supplemented; and the double-vitamin calcium carbonate composition is safe and convenient to take.
CN101190224A Vitamin B1 chewable tablets for dog or cat The invention discloses a vitamin B1 chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the prior tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 5 to 20 percent of vitamin B1.
EP2305263A1 Stabilized amorphous forms of imatinib mesylate The invention relates to the stabilized amorphous form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)-pyrimidin-2-ylamino)-phenyl]-benzamide, pharmaceutical compositions such as capsules or tablets containing this form, the use of such form in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans, and the use of formulation principles stabilizing the amorphous form of Imatinib mesylate as an intermediate for the preparation of pharmaceutical compositions.
EP1773778A1 Method for the preparation of crystal forms of torsemide in a pure state A method for the preparation of crystal form 1 of polymorphous crystalline torsemide, wherein torsemide is dissolved in an ethanol-water mixture with heating, after which the torsemide is subsequently cooled and dried once crystal separation has been performed. Drying takes place in a blade drier, for example, with the crystals being subjected to mechanical stress, wherein the crystals of crystalline form 2 are transformed into crystalline form 1.
CN101375849B Novel dosage form of sinomenine medicament or hydrochlorate thereof and preparation technique thereof The invention discloses a sinomenine or an enteric-coated controlled-release tablet of hydrochloride thereof. The prepared enteric-coated controlled-release tablet hardly releases the drug in artificial simulated gastric juice, but can slowly and smoothly release the drug in artificial simulated intestinal juice; the sustained release time of the drug can achieve more than 12 hours or even 24 hours; the enteric-coated controlled-release tablet is taken once or twice daily, the plasma drug concentration in vivo is smooth, and the peak-valley phenomenon of the plasma drug concentration is reduced; as the prepared enteric-coated controlled-release tablet hardly releases the drug in stomach, the contacted concentration of the drug with the gastric mucosa is small, the stimulation of the stomach caused by the drug is alleviated. As the prepared enteric-coated controlled-release tablet sustainedly slowly releases the drug in intestinal tract, the times of the drug administration are reduced, and the patient compliance is improved, thereby being applicable to the needs of the clinical development.
US20120046232 Compositions and methods for reducing relapse of addictive behavior Disclosed are methods and compositions comprising mGluR modulators and procysteine drugs. The methods and compositions can be used to treat subjects with prior addiction in order to reduce drug use, drug seeking or relapse.
WO2010010367A1 Solid pharmaceutical composition comprising exemestane A solid pharmaceutical composition of exemestane, in particular for oral use and treatment of cancer, comprises micronized exemestane and anti-oxidant in a film-coated tablet.
WO2009096435A1 Condensed heterocyclic derivatives and uses thereof This invention pertains to compounds represented by Formula and salts thereof, as well as medicines that are kinase inhibitors and cancer-preventing/treating agents that comprise said compounds or prodrugs thereof. [In the formula, each reference has the same meaning as in the main body of the Specification.]
US20090227606 Methods for Preventing or Treating Acute and Chronic Pain The present invention is a method for preventing or treating acute and chronic pain. Using an agent to increase the expression or activity of GLT-1, behavioral hypersensitivity is attenuated thereby preventing or treating acute and chronic pain in a subject in need of such treatment. Methods for identifying agents that prevent or treat acute and chronic pain through modulation of the expression or activity of GLT-1 or the GLT-1 pathway are also provided.
US20100009959 Pentacyclic Indole Derivatives as Antiviral Agents The present invention relates to pentacyclic indole derivatives of formula (I): wherein A, Ar, R1, R2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
CN101597229A Acetoxy-benzo-ketones compound, preparation method and application thereof The invention discloses an acetoxy-benzo-ketones compound, a preparation method and the application thereof. The compound has the right following structural formula; the preparation method comprises the whole plant of hibiscus mutabilis is dried in the air and crushed, and then is gradually processed by ultrasonic wave extraction by ethyl acetate; the extracting solution is merged and filtered; the extraction liquid is concentrated into extract which is removed pigment and fatty acid by MCI column and then passes through macroporous resin column for desugaring; after that, the product is processed by silica-gel column chromatography for primary separation, and color spectrum is prepared by high performance liquid chromatography half, so that the needed compound can be obtained; HIV-1 resistance activity screening is carried out on the compound, and the experimental result shows that the compound has good activity of HIV-1 resistance and antioxidation, the therapeutic index of HIV-1 is 86.5, and the antioxidation median elimination concentration IC 50 is 10.6 mug/L.
CN103724447A Extraction and classification method of lentinan The invention provides an extraction and classification method of lentinan. The extraction and classification method comprises the steps: sequentially carrying out drying, crushing, soaking and water extraction on Shitake mushroom to obtain crude lentinan extract firstly; then deproteinize the obtained crude lentinan extract sequentially by using chlorobenzene, calcium chloride, ammonium oxalate, trypsin and a Sevage reagent; and carrying out an alcohol precipitation method finally to prepare the lentinan. When the lentinan is extracted and prepared by using the method provide by the invention, the yield is high, the damage to the lentinan, caused by use of acid of alkaline is also avoided, the lentinan after purification has higher purity, the lentinan with different weight-average molecular weight can be obtained by virtue of classification, the molecular weight distribution range is narrower, and the lentinan has wide application prospect in the fields of organism immune regulation and tumor adjuvant therapy.
WO2007071632A3 2-pyridin-2-yl-quinazoline derivatives as potassium channel modulating agents for the treatment of respiratory diseases This invention relates to novel pyridinyl-quinazoline derivatives of formula (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. n is 0, 1, 2 or 3; X represents O, S or NR'; wherein R' represents hydrogen, alky I, cycloalkyl or cycloalkyl-alkyl; or, when n is 0 and X is NR', R' together with Y and together with the nitrogen to which they are attached form a heterocyclic ring, which heterocyclic ring may optionally be substituted with alkyl of phenyl; Y represents alkyl, cycloalkyl, alkyl-cycloalkyl, alkenyl or phenyl, which phenyl is optionally substituted one or more times with substituents selected from the group consisting of alkyl, amino-alkyl, alkyl-amino, alkyl-amino-alkyl, hydroxy-alkyl, alkoxy-alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, cyano, nitro and amino; or, when n is O, Y together with R' and together with the nitrogen to which they are attached form a heterocyclic ring, which heterocyclic ring may optionally be substituted with alkyl of phenyl; and R1, R2, R3 and R4, independently of each other, represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl; or R1 and R2, or R2 and R3, or R3 and R4, respectively, together form a benzo-fused carbocyclic ring, optionally substituted with alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl; and the remaining of R1, R2, R3 and R4 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy. alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl.
US20070281028 Drug Delivery of a Cox Inhibitor from Embolic Agents A pharmaceutical composition for malignant tumour embolisation comprises a polymer and, associated with the polymer in a releasable form, a COX inhibitor, e.g. a non-steroidal anti inflammatory drug, such as ibuprofen. The polymer is preferably-in particulate form, such as in the form of microspheres. A suitable polymer is a crosslinked polyvinyl alcohol polymer formed by the copolymerisation of PVA macromer with other ethylenically unsaturated monomers. The composition provides a synergistic treatment for the symptoms of malignant tumours, leading to tumour necrosis or ischaemia, with anti-angiogenic effects, promotion of apoptosis, decrease in invasiveness of tumour cells and resultant tumour regression.
US20080021019 immunodeficiencies, cancers, cardiovascular diseases, endocrine disorders, Parkinson's disease, metabolic diseases, tumorigenesis, Alzheimer's disease, heart disease, diabetes, neurodegeneration, inflammation, kidney disease, atherosclerosis and airway disease; substituted pyrazine compounds Disclosed is a compound of the formula: and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating protein kinase mediated diseases using the compound of formula 1.0. Also disclosed are methods of treating cancer using a compound of formula 1.0. The disclosed methods also include combination therapies wherein the compound of formula 1.0 is administered in combination with at least one addition pharmaceutically active ingredient.
WO2011047390A3 Heterocyclic benzoxazole compositions as inhibitors of hepatitis c virus This invention relates to benzoxazole compounds, compositions and devices for delivering them, processes for manufacturing them, and methods of using them in the treatment of Hepatitis C Virus.
EP1650193A2 6-Phenylphenanthridines with PDE-IV inhibiting activity Compounds of the formula I, in which R1, R2, R3, R31, R4, R5, R51, R6, R13 and R20 have the meanings indicated in the description, are novel active bronchial therapeutics.
EP1539182A1 Use of anecortave acetate for the protection of visual acuity in patients with age related macular degeneration The present invention is directed to the use of anercortave acetate or the alcohol thereof for the protection of visual acuity in patients with age related macular degeneration.
US7482372 Antiinflammatory; cartilage protecting therapeutics; antiarthritic agent; N-{4-[(2-methyl-4-quinolinyl)methoxy]phenyl}-2,4-dioxo-1,3-diazaspiro[4.5]decane-6-carboxamide; 2-(2,5-dioxo-4-imidazolidinyl)-N-{4-[(2-methyl-4-quinolinyl)methoxy]phenyl)acetamide The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.
CN102127120A Antitumor platinum(II) complex and use thereof in preparation of antitumor medicine The invention relates to an antitumor platinum(II) complex and the use of the antitumor platinum(II) complex in the preparation of an antitumor medicine. The antitumor platinum(II) complex is (N-(3-methoxybenzyl)-3-aza-1,1-cyclobutanedicarboxylic acid).(1R,2R-diaminocyclohexane)platinum(II) (hereinafter abbreviated as GS-112) of a structural formula (I) or (N-(3,5-dimethoxybenzyl)-3-aza-1,1-cyclobutanedicarboxylic acid).( 1R,2R-diaminocyclohexane) platinum(II) (hereinafter abbreviated as GS-114). The complexes of the platinum(II), namely the GS-112 and the GS-114, have high antitumor activityand can be used for preparing antitumor medicines. In addition, the result of an in-vivo acute toxicity test shows that the complexes have low toxicity, and the LD50 value of the compound is about 181.30mg/kg.
WO2013034299A1 Therapeutic uses of ectoin The invention relates to a composition comprising ectoin, hydroxyectoin and/or a salt, ester or amide of these compounds for suppression of anti-apoptotic signals to neutrophilic granulocytes and other cells involved in inflammation. The retarded apoptosis of neutrophiles is a main component for various kinds of inflammation. Administration of ectoin achieves at least partial restoration of the normal apoptosis rate, which is associated with a corresponding improvement in the inflammation symptoms.
US20120093874 Method for screening for diet providing production of milk having immunoregulatory action A method for screening for a foodstuff providing production of milk having an immunoregulatory action, a novel foodstuff having an immunoregulatory action, and a method for producing it are provided. A diet or substance that increases or decreases an amount of microRNA present in milk of a mammal is identified by using correlation of microRNA profiles in the milk and a diet ingested by the mammal or a substance contained in the diet as an index to screen for a diet or a substance providing production of breast milk having an immunoregulatory action.
CN102451324A Preparation method of bile betel nut vitamin B1 capsule The invention relates to a preparation method of a bile betel nut vitamin B1 capsule. The method comprises the following steps: 1, preparing a pig bile extract: taking fresh pig bile, adding 0.1-0.2 times sodium hydroxide, boiling for 15-18h, cooling at room temperature, adding hydrochloric acid to acidify until the pH is 3.5-4.0, washing the obtained acidic sediment with water to neutrality, filtering the sediment, drying it at 55-65DEG C, and crushing it into crude powder; 2, preparing betel nut powder: taking betel nut decoction pieces, disinfecting them in a disinfection cabinet, and crushing them into fine powder; 3, totally mixing above materials: taking the crude powder of the bile extract and the betel nut powder, adding vitamin B1 and vanillin, and uniformly mixing them; and 4, filling particles obtained after the total mixing into a capsule according to a case that 0.4g of the particles are filled into each capsule, and packaging after quality inspection qualification. The bile betel nut vitamin B1 capsule prepared with the method of the invention, which is a pure biological preparation intestinal dynamical medicine, has the advantages of intestinal peristalsis enhancement, deposited residual stool removal, bile secretion promotion, pancreas activity enhancement, fat emulsification and fat digestion absorption promotion.
CN103127163A Anxiety-relieving, depression-relieving, mood-soothing, and mental-stress-reducing composite, and preparation method and purpose thereof The invention relates to an anxiety-relieving, depression-relieving, mood-soothing, and mental-stress-reducing composite, and a preparation method and a purpose thereof. The composite comprises active components of inulin-type oligosaccharide and theanine with a ratio of 1-50:1-50.
CN101297803A Novel medical use of osthole The invention discloses an anti-gout drug of using osthole for prevention and treatment, the action target of the osthole is to inhibit xanthine oxidase, reduce the formation of uric acid salts and has stronger anti-inflammatory and analgesic effects, the prepared drug can be the osthole single component and also can be a composition containing the osthole; the drug can be prepared into tablets, capsules, granules, injection and suspension.
WO2011012883A1 Benzo [e] [1, 3 ] oxazin-4-one derivatives as phosphoinositide 3-kinase inhibitors Compounds of formula (I): wherein: W is O, N-H, N-alky!, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, -C(O)- alkyl. -C(O)-NH2, -C(O)-NH- alkyl, -SO2- alky!, -SO2-NH2 or -SO2-NH- alkyl; R2 is aryl substituted with at least one nitrogen-containing group or R2 is a nitrogen-containing heteroaryl, cycloalkyl substituted with a nitrogen-containing group, nitrogen-containing cycloalkyl, C1-C6 mono alkylamino, C1C6 bis alkylamino, C1C6 acylamino, C1-C6 aminoalkyl, mono (C1C6 alkyl) amino C1-C6 alkyl, bis (C1C6 alkyl) amino C1C6 alkyl, C1-C6-acylamino or C1 C6 alkynyl-NR11; R11 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, halogen, O-alkyl, NH-alkyl, N-dialkyl, -C(O)-R7, -C(O)-NH2, -C(O)-NH-R7, -SO2-R7, -SO2-NH2, -SO2-NH- R7, NH-acyl, NH-sulfonyl, NR7-acyl, NR7-suIfonyl, N-C(O)-NH-R7, N-SO2-NH-R7, N-C(O)-NR7R7 or N-SO2-NR7R7; and R7 is alkyl, aryl or heteroaryl, are useful as PI3K inhibitors and are useful in therapy.
CN1660176A 'Tanhuning' injection A Yanhuning injection for intravenous injection is prepared from Yanhuning through dissolving it in aseptic water, loading in ampules, sterilizing and sealing.
CN1569873A Antisense nucleic acid sequence for SARS coronavirus gene and its pharmaceutical use The invention discloses an artificial synthesized antisense nucleic acid sequence targeting coronary virogene of Severe Acute Respiratory Syndrome (SARS), which is compatible with the nucleic acid sequence on specific positioning spots on the SARS coronavirus gene, thus can block the reproduction or expression in human body or animal body and achieve the goal of treating the disease. The invention also relates to the medicinal compositions containing this antisense nucleic acid sequence, and its pharmaceutical use.
EP1313713B1 4-pyrimidinamine derivatives, pharmaceutical compositions and related methods This invention provides novel neuroprotective 4-pyrimidineamine derivatives and neuroprotective pharmaceutical compositions comprising 4-pyrimidinamines. This invention also provides methods of using these compositions to prevent ischemic cell death, particularly neuronal cell death, and reduce the likelihood of neuronal cell death in a subject due to a traumatic event. Finally, this invention provides an apparatus for administering to a subject the instant pharmaceutical compositions.
EP1091737B1 Use of 1-(3,3-diphenylpropionyl)-4-benzhydril piperazine in the treatment of pain Compounds of formula (1) wherein m is 0, 1 or 2; wherein when m is 0, Z is 0; when m is 1, Z is N, and when m is 2, Z is C; Y is H, OH, NH2, or an organic moiety of 1-20C, optionally additionally containing 1-8 heteroatoms selected from the group consisting of N, P, O, S and halo; each 1?1 and 12¿ is independently 0-5; 13 is 0 or 1; each of R?1, R2 and R3¿ is independently alkyl (1-6C), aryl (6-10C) or arylalkyl (7-16C) optionally containing 1-4 heteroatoms selected from the group consisting of halo, N, P, O, and S or each of R?1 and R2¿ may independently be halo, COOR, CONR¿2?, CF3, CN or NO2, wherein R is H or lower alkyl (1-4C) or alkyl (1-6C); n is 0 or 1; X is a linker; with the proviso that Y is not a tropolone, a coumarin, or an antioxidant containing an aromatic group and with the further proviso that if 1?3¿ is 0, neither R?1 nor R2¿ can represent F in the para position; and are useful as calcium channel blockers. Libraries of these compounds can also be used to identify antagonists for other targets.
US6890959 Such as cis-(4-dimethylaminomethyl-3-hydroxy-3-(3-methoxy-phenyl)-cyclohexanone for treatment of pain, inflammation, allergies, depression, drug/alcohol abuse, gastritis, itching, cardiovascular/repiratory diseases, epilepsy, and diarrhea Aminomethyl-phenyl-cyclohexanone derivatives of formula I or Ia, their diastereomers, enantiomers and salts formed with a physiologically tolerated acid. Also disclosed are processes for preparing the same, pharmaceutical compositions comprising the same, and methods of using the same for the treatment of pain, inflammatory reaction, allergic reactions, depression, drug abuse, alcohol abuse, gastritis, cardiovascular disease, respiratory tract disease, coughing, mental illness, epilepsy, urinary incontinence, itching, and diarrhoea.
EP2255814A1 Agent for increasing the quantity of hyaluronic acid Disclosed are a hyaluronan-increasing agent comprising at least one kind of glycerophospholipid selected from the group consisting of phosphatidylserine and phosphatidylinositol, and a skin elasticity improving agent comprising phosphatidylserine and phosphatidylinositol.
WO2014016653A1 Pharmaceutical composition comprising diamorphine for intranasal administration The invention provides a method of assembling a device and a kit suitable for administration to multiple patients comprising a multi-dose pharmaceutical composition of nasal analgesic in the form of a nasal spray. The present invention also provides a method for reducing the respiratory depressant effect associated with diamorphine administration, the method comprise a single dose pharmaceutical composition comprising lyophilized diamorphine and a diluent for reconstitution, wherein the dose of diamorphine is 0.1mg/kg body weight.
WO2011105465A1 MAILLARD REACTION INHIBITOR, α-DICARBONYL COMPOUND DECOMPOSING AGENT, AND METHOD FOR INHIBITING THE MAILLARD REACTION Disclosed is a novel Maillard reaction inhibitor producing highly effective inhibition of the Maillard reaction, and a method for using same. The Maillard reaction inhibitor has as an active ingredient at least one terpene peroxide.
CA2356745C Ionic aqueous composition containing levomenthol The invention concerns a composition in the form of an aqueous solution, in particular designed for relieving the sensation of breathing difficulties and/or promote the natural regeneration of the nose cavity mucous membrane. The invention is characterised in that it essentially consists of a levomenthol solution in an ionic aqueous solution having an osmolarity not less than that of a sodium chloride aqueous solution at 9 g/l and in which the levomenthol is dissolved, said ionic aqueous solution being selected from the group consisting of pure or diluted sea water and sodium chloride aqueous solutions optionally further containing at least one salt naturally present in sea water, the levomenthol having a concentration ranging between 10 and 250 mg/l. Said composition enables to improve the feeling of freshness provided by the levomenthol at the nose cavity cold receptors.
US20120252754 Candy Cakes Hyperkalemic Periodic Paralysis is a disease in mainly stock type horses that can be treated by giving the horse light corn syrup. Currently, the easiest way to do this is with a syringe, which is actually very difficult. The invention is a treat that will deliver a specific amount of light corn syrup per treat. This makes the entire process of delivering the corn syrup easier, faster, cleaner, and actually enjoyable for the horse. The treat can be used as an abortive measure, and also as a preventative measure if the owner incorporates the treat into the horses' daily routine. In addition to being used as the treatment for the disease, it can also be used as a regular treat for HYPP positive horses.
US20080318888 Antiproliferative activity of g-rich oligonucleotides and method of using same to bind to nucleolin Compositions and methods for modulating tumor proliferation in an individual are provided. The methods employ nucleolin-binding agents, such as aptamers. The aptamers of the present invention can be used to modulate the proliferation of malignant, dysplastic, hyperproliferative, and/or metastatic cells through interference with molecular interactions and functions of nucleolin in the tumor cell.
US20110034854 Pdt assisted vision correction and scar prevention A method and formulation are disclosed for improving the results of corneal refractive surgery, and generally reducing post-operative scarring and scarring arising from other traumas. In the vision examples, after completion of a procedure, including Photorefractive Keratotomy (PRK) or Laser-In-Situ Keratomileusis (LASIK), a photosensitizer or photosensitizer precursor is applied to the treatment site. After allowing sufficient time for the photosensitizers to accumulate among proliferating cells that occur as a result of ablation, radiation appropriate to activate the photosensitizers is administered to the treatment site. The photosensitizer is thus activated to destroy only those proliferating cells. In this way, proliferating tissue is eliminated and the cornea maintains the shape created during the surgery. As a result, instances of regression and the need for follow-up treatments, is minimized. This method is also useful for preventing post-surgical scarring that can lead to vision problems such as corneal haze. Likewise the method and formulations, presented here, are suitable for reducing post-operative scarring, and trauma cased scarring in general. For such scars, a photosensitizer or photosensitizer precursor is topically applied to the treatment site. After allowing sufficient time for the photosensitizers to attach to proliferating cells, radiation appropriate to activate the photosensitizers is administered to the treatment site. The photosensitizer is activated to destroy only those proliferating cells.
EP1829542A1 Peroxisome proliferator-activated receptor (ppar) activator and drug, supplement, functional food and food additive using the same The present invention provides a peroxisome proliferator-activated receptor (PPAR) activator, which is free from the problem of side effects, can be taken over a long term and has no characteristics taste. Nobiletin is employed as a PPAR activator. Nobiletin has an excellent PPAR activity and has an excellent adiponectin secretion-promoting effect, and is contained in a large amount in citrus fruits, in particular, in Shiikuwasha (Citrus depressa HAYATA) indigenous to Okinawa (Japan). Since citrus fruits have been consumed for many years, the safety of nobiletin has been proven and besides, nobiletin has a low calorie content. Therefore, it can be taken over a long term. Moreover, because of being tasteless and odorless, nobiletin would not damage the unique taste of a food when added thereto. Therefore, it can be added to foods and taken.
US20060211760 Indolamide derivatives which possess glycogen phosphorylase inhibitory activity A compound of the formula (1) or a pharmaceutically-acceptable salt wherein, for example, A is phenylene or heteroarylene; Y is selected from —C(O)R2, —C(O)OR2, —C(O)NR2R3, -(1-4C)alkyl [optionally substituted]-(2-4C)alkenyl, —SO2NR2R3, and —S(O)cR2 (wherein c is 0, 1 or 2); compounds which possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
US20120288579 Use of lignan compound for anti-wrinkle treatment The present invention relates to a novel use of lignan compounds, which are isolated and purified from nutmeg or the aril of nutmeg for anti-wrinkle, and more particularly, the present invention relates to a novel use for anti-wrinkle of an extract of the nutmeg or an extract of the aril of the nutmeg, fragrin A, austobailignan 7, licarin E, and macelignan. The extracts and lignan compounds of the present invention have activities in suppressing collagen degradation enzyme-1 (MMP-1, matrix metalloprotei-nase-1) and formation of new collagen (type-1 procollagen), thereby having effect on inhibitng wrinkle caused by photoaging. Accordingly, the extracts and lignan compounds of the present invention may be useful for preventing or treating wrinkle caused by photoaging.
US20110217390 Method of manufacturing digestible powder that generates hydride ion (H-) A method of manufacturing digestible powder that generates a hydride ion (H−) when dissolved in water is provided. A vacuum oven system that can reach 600° C. and 10−5 torr is used within this method. The method according to this current application comprises of ten to eleven steps of vacuuming, heating and hydrogen treatment of coral reef powder. By adding mixtures of magnesium, phosphorus and potassium, the maximum treating temperature and vacuum pressure is lowered. The coral reef powders treated via the ten steps emit hydrogen when dissolved in the water like powders that are treated with a mixture of natural form of magnesium, phosphorus and potassium complex. Those natural form of the magnesium, phosphorous and potassium includes (NH4)MgPO4.6H2O (struvite), MgSO4.KCl.H2O (Kainite), K2SO4.MgSO4.6H2O (Schonite), K2SO4.MgSO4.4H2O (Leonite), and K2SO4.2MgSO4 (Langbeinite).
WO2006035286A2 Process for preparating enantiomerically pure fluvastatin sodium and a novel polymorphic form thereof The present invention provides processes for preparing enantiomerically pure fluvastatin sodium. The present invention also provides pharmaceutical compositions comprising the enantiomerically pure fluvastatin sodium for antagonizing HMG-CoA. In addition the present invention provides a novel polymorphic form of enantiomerically pure fluvastatin sodium.
CN101313912A Application of echinacoside in preparing medicament for treating parkinsonism The invention relates to an application of echinacoside in the preparation of drugs for treating Parkinson's disease. The invention discloses that echinacoside has a remarkable protective effect against the MMP+ mediated cell injury. The echinacoside can be used to prepare drugs for the treating Parkinson's disease and offers a new treatment for people with the Parkinson's disease.
US7879993 Platelet derived growth factor (PDGF) nucleic acid ligand complexes This invention discloses a method for preparing a complex comprised of a PDGF Nucleic Acid Ligand and a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound by identifying a PDGF Nucleic Acid Ligand by SELEX methodology and associating the PDGF Nucleic Acid Ligand with a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound. The invention further discloses Complexes comprising one or more PDGF Nucleic Acid Ligands in association with a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound. The invention further includes a Lipid construct comprising a PDGF Nucleic Acid Ligand or Complex and methods for making the same.
CN102633852A Imine stigmasterol derivative and application thereof in anti-cancer drug The invention discloses an imine stigmasterol derivative and application thereof in an anti-cancer drug. The chemical structural formula of the imine stigmasterol derivative is shown in the specification, wherein the group represented by R1 is defined in the specification. The in-vitro cancer cell inhibition test indicates that: the imine stigmasterol derivative disclosed by the invention has an obvious inhibition effect on multiple tumor cells such as human breast cancer cell strain (MCF-7), human lung cancer cell strain (A549), human liver cancer cell strain (HepG2) and the like, and shows relatively low toxicity against normal cells; and particularly, the imine stigmasterol derivative has strong cell toxicity against MCF-7, wherein the toxicity is over 3 times that of phytosterol. The imine stigmasterol derivative disclosed by the invention can be used for preparing a drug for treating cancer.
WO2012128576A2 Composition for treating lower or damaged cognitive function containing dehydroglyasperin c typically found in licorice Provided are a pharmaceutical composition and a food composition, which can be utilized to protect brain cells and improve cognitive function, due to the confirmed activity of dehydroglyasperin C, which is one licorice ethanol extract, for suppressing neuronal apoptosis.
CN1743328A Hexahydro-pyrazino-pyridino-indole, and its systhesis and use As shown in the general formula I of the compound at right, R is among H, -CH3, -CH(CH3)2, -CH2COOH, -CH2C6H5, -CH2OH, -CH2(CH2)3NH2 and indole-3 radicle-methylene. The synthetic method is as follow: first, with sulphuric acid as catalyser, let tryptophan react with methanal to generate (3S)-1, 2, 3, 4-tetrahydro-beta-carboline-3- carboxylic acid which then react with SOCl2 and methanol to generate (3S)-1, 2, 3, 4-tetrahydro-beta-carboline-3-carbomethoxylate; then, with the presence of N-hydroxyl benzotriazole (HOBt) and DDC(N, N-bicyclohexyl), let Boc-amino acid(butyloxycarbonyl-amino acid) to react with (3S)-1, 2, 3, 4-tetrahydro-beta-carboline-3-carbomethoxylate to generate N-butyloxycarbonyl-amino acyl-1, 2, 3, 4-tetrahydro-beta-carboline-3-carbomethoxylate, which will be cyclized, in HCl/ethyl acetate solution, into hexhydro-pyrazino-pyrrolo-didone; in the end, hexhydro-pyrazino-pyrrolo-didone is reduced into hexhydro-pyrazino-pyrrolo-didone by potassium borohydride. The compound of formula I possess antihistamine activity.
CN102824381A Isatis root and vitamin C tablet and preparation method thereof The invention discloses an isatis root and vitamin C tablet and a preparation method thereof. The isatis root and vitamin C tablet consists of the following components in parts by weight: 100-500 parts of isatis root micro powder, 100-300 parts of vitamin C, 4-20 parts of binding agent and 9-32 parts of lubricating agent, wherein the binding agent comprises hydroxypropyl methyl cellulose and povidone, and the lubricating agent comprises silica and magnesium stearate. The invention also provides the preparation method for the isatis root and vitamin C tablet. The isatis root and vitamin C tablet prepared through the components in parts by weight and the corresponding preparation method has double effects of the isatis root and the vitamin C and is very good in effect of preventing and curing diseases. Meanwhile, the isatis root and vitamin C tablet is excellent in quality, long in quality guarantee period and simple in process.
US20120136023 Inhibitors of HIV Replication The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication.
US20060241151 Pyrid-2-one derivatives and methods of use Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also realtes to processes for making such compounds as well as to intermediates useful in such processes.
WO2006084854A2 [1,2,4]-dithiazoli(di)ne derivatives, inducers of gluthathione-s-transferase and nadph quinone oxido-reductase, for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]- dithiazolidine-3,5-diylidene-diamine derivatives as inducers of glutha-thione-S- transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament useful in the for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein the symbols have the meanings given in the specification.
EP1648874A2 Piperazine derivatives and their use as therapeutic agents Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
WO2007037555A1 Therapeutic or diagnostic application of dusp15 gene It is intended to provide a therapeutic agent for cancer containing an expression inhibitor or activity inhibitor of DUSP15 protein; a method for screening a compound which can be used as an active ingredient of such a therapeutic agent; an antibody against the DUSP15 protein; a diagnostic agent for cancer/a diagnostic method for cancer using the antibody and the like.
CN1943728A A first-aid medicine for treatment of tetanus and lyssodexis This invention relates to the first-aid medicine for treatment of tetanus and lyssodexis. It provides a combined internal and external medicine which uses the combined medical effect of multi-herbal medicine to treat tetanus and lyssodexis so to reach the aim of the first-aid of the tetanus and lyssodexis. The medicine is composed by the using 6 grams of each of the following medical ingredients: jackinthepulpit tuber,radix saposhnikoviae,Dahurian angelica root,tall gastrodia tuber, Incised notopterygium root, giant typhonium tuber, cut the above ingredients into pieces, taking again 30 grams of slightly baked isinglass,30 grams of hangfen(baked to yellow colour), 30 grams of bentonite alum(stir-fried to red colour) and 9 grams cinnabar and have the rolled into fine powders, then use hot alcohol to prepare the medicine by using the above medical ingredients and the rolled fine powders.Becaouse the cost of the above medical ingredients of this compostion is low, it can be used as the family standby medicine, once one is stabbed or bite by a dog, he or she can immediately externally daub the medicine to the hurt, and swallow the medicine internally. This not only can safe the patient but also help to save the time if the case is serious.
US20120058968 Composition containing fermantable polysaccharides The present invention relates to a composition to a nutritional composition comprising 0.1 to 15 gram fermentable partially hydrolysed gum having a degree of polymerisation between 10 and 300 per 100 gram dry weight of the composition and 0.1 to 15 gram fermentable, indigestible polysaccharide other than a hydrolysed gum having a DP between 10 and 300 per 100 gram dry weight of the composition.
CN102351787A High-bioavailability roflumilast compound The invention belongs to the technical field of medicines, and particularly relates to a roflumilast compound shown in formula I and a preparation method thereof. Roflumilast is a new crystal form, and has the advantages that the chemical purity is high, the highest purity content is smaller than 1 per mill, the optical purity is high, roflumilast is soluble in water, and a preparation prepared from roflumilast has good stability, particularly wet stability, and high bioavailability. The compound provided by the invention has low production cost and stable quality, and is suitable for industrial production.
CN102920661A Preparation method of water-soluble isofraxidin mixed powder The invention discloses a preparation method of water-soluble isofraxidin mixed powder, which is characterized in that isofraxidin is dissolved in organic solvent in appropriate proportion to get isofraxidin solution, then the isofraxidin solution is slowly infused into mannitol aqueous solution in the process of homogenization, which is 3-15 times in volume of the isofraxidin solution, the mixed liquid is homogenized to homogeneous emulsion by a homogenizer with the rotational speed of 5,000-20,000 revolutions per minute at the temperature of 4-40 DEG C, the organic solvent is removed at the temperature of 30-100 DEG C, and epigranular and fine nano-powder is obtained through lyophilization. The isofraxidin mixed powder obtained through the preparation method is homogeneous, water-soluble, high-yield, cost-efficient and easy to be industrialized.
CN101297799A Arotinoid ethylester for curing acne The invention provides a new drug-arotinoid ethylester for the treatment for skin diseases and acnes. The arotinoid ethylester for the treatment for acnes has the advantages of small dose, strong efficacy, good safety and greater economy.
EP1968975A2 Tylophorine analogs as antitumor agents Compounds of Formula (I) are described: preferably subject to the proviso that either (a) R2 and R3 together form -O-CH(R10)-O-, or (b) R5 and R6 together form -O-CH(R10)-O-, wherein R10 is H, halo, or loweralkyl. Pharmaceutical salts, formulations, and methods of using the same in the treatment of cancer are also described.
CN101428011A Inhalation powder spray for treating respiratory diseases such as chronic obstructive pulmonary disease and asthma The invention discloses powder inhalation for treating respiratory system diseases such as chronic obstructive pulmonary diseases and asthma. The powder inhalation comprises all the tautomer, enantiomer, stereoisomer, acid anhydride, acid addition salt, basic salt, solvolyte, analogue and derivative of a first active ingredient - ipratropium, a second active ingredient - salbutamol, and one or more pharmaceutically acceptable carriers; wherein other pharmaceutically acceptable salt of salbutamol is selected from other salt of organic acid of salbutamol sulfate or salbutamol, and the mass ratio of the first active ingredient and the second active ingredient is 1:10 to 15:1; according to the ratio of the prescription, uniformly blending the ipratropium and the salbutamol and crushing to an average grain size of 1 to 5 Mum, crushing the dried carrier to an average grain size of 1 to 5 Mum, and filling the uniformly blended powder into a filling machine to produce the powder inhalation. The powder inhalation can directly act on the affected part, the efficacy presents quickly, and the use is convenient.
CN101032566A Powder for external application for defervescence The present invention discloses one kind of externally applied fever allaying medicine powder, which is prepared with gypsum 1.5-2.5 weight portions, alum 1.5-2.5 weight portions, sweet wormwood 0.5-1.5 weight portions, cape jasmine 1.5-2.8 weight portions, rhubarb 1.5-2.8 weight portions, weathered sodium sulfate 0.5-1.5 weight portions, and through crushing, grinding, sieving, mixing and packing. The externally applied fever allaying medicine powder is used in treating heat diseases via being mixed with egg white and applied to local skin, and has fast acting, reliable curative effect and other advantages.
WO2013108837A1 Pyrazole derivative with tlr inhibiting properties The objective of the present invention is to provide a novel compound that inhibits at least one type selected from the group consisting of TLR3, TLR7 and TLR9, and that has excellent preventive and therapeutic effects on autoimmune diseases, inflammations, allergies, etc. A compound represented by general formula (1) or a salt thereof, or a solvate thereof. [In the formula: rings W and Z are 5 to 7 membered saturated or partially unsaturated nitrogen-containing heterocyclic groups; T is a C1-6 alkyl group which may be substituted with an oxo group; ring Y is a group represented by formulas (2), (3) or (4); (2) (3) (4) X1, X2 and X3 are C-R7 or nitrogen atoms, wherein X1 and X2 are not simultaneously C-R7; R7 is a hydrogen atom, a halogen atom, a hydroxyl group, etc.; S and U are single bonds or N-R8; R8 is a hydrogen atom or a C1-6 alkyl group; V is a hydrogen atom, a C1-6 alkyl group, a C6-10 aryl C1-3 alkyl group, a 3 to 7 membered saturated heterocyclic group, etc.]
WO2010127210A1 Method of reducing intraocular pressure in humans Provided herein are compounds of Formula I, compositions comprising an effective amount of a compound of Formula I, and methods for reducing intraocular pressure comprising administering an effective amount of compounds of Formula I to a subject in need thereof.
US7199137 Treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy Novel compounds (I) and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy wherein Ar is a group of formula a) or b).
US20120021000 HIV DNA Vaccine Methods of Use The present invention is directed to a DNA vaccine for immunization against HIV. The invention comprises a DNA molecule that has a sequence encoding a plurality of viral proteins capable of stimulating an immune response against HIV. The DNA molecule is rendered safe for use as a vaccine by the disruption of genes encoding reverse transcriptase, integrase, and Vif. The DNA molecule is further rendered safe by at least a partial deletion of the 3′ LTR.
US20120183593 Hydrogels used to deliver medicaments to the eye for the treatment of posterior segment diseases This invention provides a polymeric drug delivery system including a hydrogel containing one or more drugs for the treatment of a posterior segment disease. Allowing passive transference of this drug from a dilute solution into the hydrogel produces the delivery system. The hydrogel, when placed in contact with the eye, delivers the drug. The delivery of the drug is sustained over an extended period of time, which is of particular utility in the eye, which is periodically flushed with tears. This sustained delivery accelerates the treatment process while avoiding potential damaging effects of localized delivery of high concentrations of compounds, e.g., from eye drops.
US7122525 Targeted therapeutics and uses thereof The invention features a method of delivering a drug to a diseased cell by linking the drug to a rifamycin derivative, compositions that include drug-rifamycin conjugates of the invention, and methods for treating disease using those compositions.
WO2013107761A1 Substituted triazoles and their use for treatment and/or prevention neurological and psychiatric disorders This invention relates to compounds of formula (I), their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
US20100152186 Triazolyl pyridyl benzenesulfonamides Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.
WO2012168817A1 Pyrazolo[3,4-d]pyrimidine compounds and their use as pde2 inhibitors and/or cyp3a4 inhibitors The present invention provides, inter alia, compounds of Formula (I) and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal. The present invention further provides compounds of Formula (Id) and pharmaceutically acceptable salts thereof as CYP3A4 selective inhibitors.
WO2009020990A1 2- [ (2-{phenylamino}-1h-pyrrolo [2, 3-d] pyrimidin-4-yl) amino] benzamide derivatives as igf-1r inhibitors for the treatment of cancer Novel pyrrolopyrimidines as shown in formula (I) and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.
CN103623162A Traumatic injury treatment paste and preparation method thereof The invention discloses traumatic injury treatment paste. The paste is prepared from the following raw materials: raw monkshood, raw radix aconiti agrestis, raw pinellia ternate, raw semen strychni, paris polyphylla, Yunnan alpine yarrow herb, high-quality pepper, kadsura root-bark, cinnamon, semen brassicae, asarum, Chinese azalea flower, radix euphorbiae lantu, flos daturae, Sichuan pepper, pericarpium zanthoxyli, camphor, frankincense, myrrh, native copper, ground beetle, safflower, divaricate saposhnikovia root, herba schizonepetae, mulberry twig, geranium wilfordii, horn meal, rubia cordifolia, dog bone, and musk. The preparation method comprises the following steps: preparing the raw material components; grinding the dog bone and the musk jointly to obtain fine powder; grinding the camphor and borneol jointly to obtain fine powder; jointly grinding other drug components into fine powder; melting arbitrary one of medical Vaseline, propolis, rosin and other paste matrix in a stone pot, adding the medicinal powder in a stirrer, and uniformly stirring; adding the fine powder of dog bone and musk and the fine powder of camphor borneol. The traumatic injury treatment paste has a prominent curative effect in traumatic injury, rheumatism, spinal stenosis, hyperostosis, ligamentous injury, sprain and the like, and prevents relapse.
EP1792611A1 Matrix controlled transdermal system for stable derivatives of ACE inhibitors In a transdermal therapeutic system (TTS) comprising an impermeable backing layer, one or more matrix layers and a removable backing layer, the matrix layers contain active agent(s) (A) consisting of a dicarboxylic acid angiotensin converting enzyme (ACE) inhibitor which has been derivatized to give a diester, a di-salt with base(s) or a mono-salt with acid(s). In a transdermal therapeutic system (TTS) comprising an impermeable backing layer, one or more matrix layers (where at least one of the layers is self-adhesive or a separate adhesive layer is provided) and a removable backing layer, the matrix layers contain active agent(s) (A) consisting of a dicarboxylic acid angiotensin converting enzyme (ACE) inhibitor which has been derivatized to give a diester, a di-salt with base(s) or a mono-salt with acid(s).
US20080206266 Carbohydrate ligand that specifically binds to a leczyme; nucleic acid sequence encoding a nonclassical MHC class I heavy chain; ability to associate with a beta 2 microglobulin; major histocompatibility complex transplantation molecules The present invention provides a substantially purified carbohydrate ligand that specifically binds to a leczyme. The invention also provides methods to identify a carbohydrate ligand that specifically binds to a leczyme or a leczyme that specifically binds to a carbohydrate ligand. The invention further provides methods to identify a peptide that binds to the carbohydrate ligand binding site of a leczyme. The present invention provides methods to isolate a carbohydrate ligand or a leczyme and to identify a carbohydrate ligand or a leczyme that modifies the function of a cell and to obtain such functionally modified cells. The invention further provides methods to modify a cell to express a carbohydrate ligand by introducing an expression vector encoding a leczyme into the cell. The invention also provides methods to modulate the immune response to an antigen by administering the antigen and a carbohydrate ligand. In addition, the invention further provides methods to treat a disease state involving a leczyme by administering a carbohydrate ligand that binds the leczyme or by administering a leczyme that has a similar binding specificity to the leczyme involved in the disease state. The invention further provides methods to diagnose a genetic basis for hemochromatosis by detecting a mutation in a class I MHC molecule that reduces it's ability to associate with β2 microglobulin.
CN101380301B Compound doxycycline hydrochloride injection for animals and preparation method thereof The invention relates to a compound doxycycline hydrochloride injection for veterinary use and a preparation method thereof. The raw materials comprise doxycycline hydrochloride, thiamphenicol, dexamethasone sodium phosphate, trimethoprim, diclofenac sodium, organic solvent and water for injection. As a special compound preparation for veterinary use, the injection has obvious curative effects oninfectious diseases caused by gram-positive bacteria, gram-negative bacteria and mycoplasma, quickly takes effects after the injection is injected into livestock with the diseases, and has special efficacy on mixed infection and severe diseases caused by various pathogenic bacteria and viruses. After intramascular for animals, the injection is easily absorbed, takes effect for a long time and causes little local stimulation. The injection has the advantages of convenient use, short treatment course, low drug resistance, and the like.
US20120171293 Granulated material mixture comprising two different granulated materials for artificial callus distraction A granulate mixture suitable for regenerating a bone contains at least one expandable particle and at least one nondeformable particle. The at least one expandable particle contains a swelling agent. The swelling is enclosed by a biodegradable sheathing or be a biodegradable casing. Three-dimensional callus distraction may be accomplished by introducing the granulated mixture into a bone defect.
EP2552919A1 Aryl-cyclohexyl-tetraazabenzo[e]azulenes The present invention is concerned with aryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I, wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in particular as Via receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
CN102119918A Medicinal sustained-release preparation for treating osteomyelitis and preparation method and application thereof The invention discloses a medicinal sustained-release preparation for treating osteomyelitis and a preparation method and application thereof. The medicinal sustained-release preparation is prepared by compressing poly DL-lactic acid (PDLLA) and levofloxacin in a ratio. The preparation method comprises the following steps of: A, cutting the PDLLA, placing the PDLLA together with levofloxacin powder with corresponding mass into an organic solvent, and mixing at a constant speed until the PDLLA and the levofloxacin powder are dissolved; B, heating a blend in an oven so as to volatilize the organic solvent, and scraping off the dried blend from the wall of a container; C, cutting the blend into proper blocks, and placing into a metal mould for primary compression, so that the blend blocks are closely combined into a whole; D, heating the mould and the blend in the mould together in the oven, compressing the mould for forming, taking the mould out, putting the mould into a latex glove and putting into tap water for cooling, and demoulding to obtain a blend medicinal tablet of the PDLLA and the levofloxacin; and E, packaging the medicinal tablet by using a plastic bag, and sterilizing by using 60Co25KGy. The method is easy to realize, and the medicinal sustained-release preparation is convenient to take, has an obvious treating effect, high safety and long medicinal effect time, and is suitable to prevent and treat acute and chronic osteomyelitis.
CN102225059A Application of mannitol in preparing antitumor medicines The invention discloses an application of mannitol in preparing antitumor medicines, and particularly relating to an application of a mannitol injection of a specific concentration (10-19%) in treating lung cancer, liver cancer, breast cancer, pancreatic cancer, stomach cancer, adenocarcinoma of stomach, and so on. Traditionally, mannitol is only used as a diuretic, a high-penetration antihypertensive agent, and so on. The inventor finds that mannitol has antitumor activity through scientific experiments, confirms that by using a multiterm apoptosis detection technique and detecting apoptosis-associated genes bc1-2 and bax, mannitol of a specific concentration can induce distinct apoptosis of a great variety of cancer cells, and masters the effect relationship between concentration and time, and preliminarily elucidates the possible mechanism. In addition, the inventor applies the research results in treating tumor patients and obtains distinct curative effects. The results in the invention provide theoretical basis and practical cases for the application of mannitol in preparing antitumor medicines and the clinical applications of mannitol.
CN101260077B Quinolin-2-ones derivative, pharmaceutical composition and use thereof The invention discloses a formula (I) compound 6-chloro-3-(2-ethoxyl)-quinoline-2-ketone, a drug combination which contains the formula (I) compound, is used to treat hepatitis B and consists of 6-chloro-3-(2-ethoxyl)-4-phenylchinoline-2-ketone or 6-chloro-3-(2-ethoxyl)-4-(2-fluoro-phenyl)-quinoline-2-ketone or 6-chloro-3-(2-ethoxyl)-4-(2-chloro-phenyl)-quinoline-2-ketone and a pharmaceuticallyaccepted carrier, preparation methods for the three drug compounds, and applications thereof in the preparation of anti-hepatitis B inhibitor drugs and drugs for treating hepatitis B.
US20080051350 inulin sulphate for treatment or prophylaxis of arthritis, osteoarthritis The present invention relates to the use of a sulphated polysaccharide in acid form or as a physiologically acceptable salt thereof, selected from the group consisting of inulin sulphate, gellan sulphate, pullulan sulphate, curdlan sulphate, alginiq acid sulphate, laminarin sulphate, and pectin sulphate, for the preparation of a medicament for the treatment or prophylaxis of arthrosis in a mammal. Preferably, the sulphated polysaccharide is inulin sulphate, most preferably inulin polysulphate sodium salt. The present invention also relates to the use of a sulphated oligosaccharide derived from a polysaccharide selected from the group consisting of inulin, gellan, pullulan, curdlan, alginic acid, laminarin, and pectin, for the preparation of a medicament for the treatment or prophylaxis of arthrosis in a mammal.
CA2191746C [a]-annelated pyrrole derivatives and pharmaceutical use thereof The present invention relates to heterocyclic compounds of the formula (see formula I) in which R1-R7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.
US7906150 Preparation derived from shark cartilage for treatment of diseases related to excessive PHF or excessive intracellular calcium Shark cartilage extract has been shown to be an antagonist of parathyroid hypertensive factor (PHF). In view of this, shark cartilage extract can be used to treat conditions related to excessive PHF activity. Such diseases include hypertension and some other diseases related to intracellular calcium elevation. Methods for producing the shark cartilage extract and methods for administering the extract are disclosed.
WO2013158616A1 Treatment of medium-chain acyl-coa dehydrogenase deficiency The present invention provides for methods and compositions for treating medium chain acyl-CoA dehydrogenase deficiency. It is based, at least in part, on the discovery that phenylbutyrate can serve as a substrate for medium chain acyl-CoA dehydrogenase. In non-limiting embodiments, phenylbutyrate and/or another source of phenylacetate is administered as a chaperone treatment to patients suffering from medium chain acyl-CoA dehydrogenase deficiency.
CN103655607A Pharmaceutical composition containing omeprazole The invention belongs to the technical field of medicine, and provides a pharmaceutical composition containing omeprazole. The pharmaceutical composition comprises 0-10 parts by weight of a disintegrating agent, 1,000-1,600 parts by weight of sodium bicarbonate and 20-50 parts by weight of omeprazole and glyceryl behenate. The pharmaceutical composition provided by the invention is suitable for mass production, and is high in stability.
US20070254956 Medicament for Therapeutic and/or Preventive Treatment of Restenosis or Reocclusion After Vascular Recanalization Operation A medicament for therapeutic and/or preventive treatment of restenosis or reocclusion after a vascular recanalization operation, which comprises as an active ingredient a compound represented by the following formula or a physiologically acceptable salt thereof, and a medical device for an intravascular treatment, which contains said compound or the physiologically acceptable salt thereof in a releasable form.
CN103420980A Dabigatran derivatives The invention aims to provide dabigatran derivatives, which are presented by the formula I with anticoagulant activity, optical isomers, and medicinal salts thereof. R1 represents H or alkyl group with a carbon number between 1 and 3, R2 represents R3 or -OR3, and R3 represents an alkyl group with a carbon number between 1 and 8 or a naphthenic group with a carbon number between 3 and 8.
US6869968 Such as 3-(4-fluorophenyl)-4-(4-methysulphonylphenyl)-2-(3H)-oxazolone; for treating colorectal cancer, fevers, and inflammation The invention relates to 2-(3H)-oxazolone derivatives. They may be used as COX-2 inhibitors. The compounds may be used in the treatment of colorectal cancer.
CN101240037A Jelly fungi heptasaccharide and its preparation technique and application Agaric heptasaccharide, preparation and application thereof. Production of black fungus nationwide reaches 60-70 thousand tons according to estimation. But further processed product of agaric is not much. Preparation and application of agaric oligosaccharide is not published yet. Agaric heptasaccharide, with a appearance of white or light yellow solid powder, is easy to absorb moisture, containing 6 mannose connected by alpha-(1-3) glycosidic bond in molecule, and with the second mannose connected with xylose by (3-1) glycosidic bond, represented by formula above. The inventive product can be used as medicament.
CN101440118A Saponin compound extracted from Momordica grosvenori root, preparation and use thereof The invention relates to the medicine technical field, in particular to saponin compounds of Siraitic acid IIB and Siraitic acid IIC which are extracted and separated from fructus momordicae roots, a method for preparing the same and application thereof in an anti-tumor medicine. The molecular formulas of the two compounds are C40H60O14 and C41H62O15 respectively. By various modern spectral analysis, particularly the application of advanced two-dimensional nuclear magnetic resonance spectrum to comprehensive analysis, the chemical structures of the two compounds are determined. In vitro anti-tumor tests show that the compound Siraitic acid IIB can obviously inhibit lung cancer cells A-549 and liver cancer cells Hep-G2, and the compound Siraitic acid IIC can also obviously inhibit liver cancer cells Hep-G2. The invention provides lead compound for research on a new anti-tumor medicine, and has essential values in comprehensively developing and utilizing fructus momordicae resources.
EP2227474A1 Azo and diaza derivatives and uses thereof in phototherapy The invention relates generally to optical agents, including Type 1 phototherapeutic agents, for biomedical applications, such as phototherapy. Provided are fused ring azo and diaza compounds comprising a plurality of fused rings including a first ring having an intra-ring azo or intra-ring diaza group capable of activation upon exposure to electromagnetic radiation in visible and/or infrared regions of the electromagnetic spectrum. Optical agents of the invention enable a versatile phototherapy platform for treatment of a range of pathological conditions, including the treatment of cancers, stenosis and inflammation. The invention further provides preparations and formulations comprising the fused ring azo and diaza compounds and methods of making and using the fused ring azo and diaza compounds as optical agents in in vivo or ex vivo biomedical procedures.
CN103372016A Application of Chukrasone A in preparation of medicines for lowering blood glucose The invention discloses an application of Chukrasone A in the preparation of anti-diabetic medicines. The application of the Chukrasone A has the advantages of providing bran-new choice and idea for the existing anti-diabetic medicines, widening the choice field of the anti-diabetic medicines and contributing to the development of the technical field. The application of the Chukrasone A is proven to have an obvious anti-diabetic effect. The Chukrasone A is a compound with a definite chemical structure. The application of the Chukrasone A in the preparation of the anti-diabetic medicines is disclosed for the first time. As the skeleton type of the Chukrasone A belongs to a bran-new skeleton type and the Chukrasone A has unexpected strong activity on the prevention and treatment of diabetes, the possibility that other compounds provide revelation does not exist. The Chukrasone A has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for treating the diabetes.
CN101292982A Enoxacin freeze-dried powder needle composing prescription and preparation technique The invention discloses a prescription of enoxacin freeze-dried powder injection and a preparation technique thereof, belonging to the field of the medicine technology. The prescription of the enoxacin freeze-dried powder injection essentially consists of the enoxacin, cosolvent and excipient; the preparation technique includes four steps as liquid preparation, medicinal carbon adsorption, filtration and freeze-drying. The method has the advantages of being easy to operate, simple technique, low production cost, stable product quality and being easy to transport and store.
EP1118659B1 Expression systems for functional nucleic acid expression Ribozymes containing the base sequence (I) or nucleotide sequence (II).
CN102727494A External application drug composition for treating fungus infection of skin In the prior art, squalene cyclooxygenase inhibitors provide unobvious itching relieving effects for treatment of fungus infection. In order to over the disadvantage of the squalene cyclooxygenase inhibitors, the present invention provides an external application drug composition containing a squalene cyclooxygenase inhibitor and an H1 receptor blocker, wherein the drug composition has characteristics of fungus killing, synergistic anti-inflammatory and synergistic itching relieving, and symptoms of fungus infection of superficial skin can be significantly improved with the drug composition.
CN1778299A Cavitas nasisal cavity medicine-supply preparation with radix aconiti agrestis methyl A snuff of aconitin A for treating pain and inflammation is prepared from aconitin A and the pharmacologically acceptable excipient.
CN102219812A Tumor targeting deoxyglucose composite drug and preparation method thereof The invention relates to the field of drug synthesis and applications, in particular to tumor targeting deoxyglucose composite drug and a preparation method thereof. The drug can improve effective drug concentration at tumor parts and reduce toxic and side effects. Amino of doxorubicin or nimustine is modified by deoxyglucose with a targeting function and certain anti-tumor effect, thus achieving targeting administration, reducing toxic and side effects of doxorubicin and nimustine, improving effects on tumor treatment and the like and further playing a role in synergy effect on tumor resistance. The deoxyglucose-doxorubicin composite drug or deoxyglucose-nimustine composite drug is prepared by taking deoxyglucose and doxorubicin or nimustine as main raw materials and succinic anhydride as link bodies and adopting a covalency connection method, thus having targeted treatment action on the tumor.
WO2013086515A1 Compositions and methods for the prevention or treatment of diabetic complications The invention provides compositions and methods for the prevention, amelioration, and/ or treatment of diabetes complications, including ocular diseases associated with increased glucose transport and/or oxidative stress.
EP2481398A1 Slow-release cilostazol tablet having an improved elution rate and minimal side effects Provided is a slow-release tablet including cilostazol as a pharmacologically active component, which is efficacious in suppressing aggregation of blood platelets and promoting vascular relaxation by inhibiting phosphodiesterase types. The slow-release cilostazol tablet has an extended elution time so that the slow-release cilostazol tablet can be taken once daily for convenience of drug use, and minimizes the manifestation of headache which is one side effect caused when women, the elderly and children take conventional cilostazol preparations so that the convenience of drug use can be improved. Also, the slow-release cilostazol tablet exhibits a stable elution pattern with no variation in elution rate according to changes in pH in the stomach and intestines, as well as an effect of delaying the release of a drug, using a mixture of hydroxypropyl methylcellulose and a carbomer as a release-controlling polymer.
CN1994309A Use of caryophyllene compound composition in medicine for treating general anxiety neurosis and depression The invention relates to a drug which uses betula oil caryophyllene benzalacet aldehyde, 2-methoxy benzalacet aldehyde, and acetic acid benzalacet aldehyde, as main active components to treat depression, etc. The invention can treat significant body representation. And it can be extracted from traditional drug or synthesized artificially. It has simple components and wide resource.
CN102961364A Sensitive and color-changing anti-acne repairing diaphragm The invention provides a sensitive and color-changing anti-acne repairing diaphragm which is a transparent sheet body, wherein the sheet body internally contains a plurality of dispersed particles which contain sensitive and color-changing components and anti-acne components and can be applied to the face, the abdmen-thorax part, the back, the hip and the four limbs. The sensitive and color-changing anti-acne repairing diaphragm contains the anti-acne components, can be used for enhancing the effect of eliminating acnes during laser therapy, and can be used for reducing burning heat sensation of the skin during laser therapy and lightening side effects of gall and the like during laser therapy because of a wet jelly body. In addition, the sensitive and color-changing anti-acne repairing diaphragm contains the sensitive and color-changing components, a part subjected to laser treatment generates a color-changing effect, and a laser part is evaluated by a patient or doctor through visual inspection after being subjected to the laser treatment.
US7176203 Imidazo-triazine derivatives as ligands for gaba receptors A class of imidazo[1,2b][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
US7317114 Process to obtain dibenzylbutyrolactonic lignans, process to obtain synthetic derivatives from lignans bearing anti-Chagas chemoprophylactic and therapeutical activities The invention refers to a process to obtain lignans, especially to obtain cubebin and methylpluviatolide from leaves of Zanthoxylum naranjillo or Piper cubeba. It also refers to a process to obtain semi-synthetic derivatives of cubebin, especially dibenzylbutirloactonic lignans, such as: hinokinin, o-acetyl cubebin, o-methyl cubebin, 6,6′-dinitrohinokinine and o-dimethylethylamine cubebin and other derivatives which may be obtained, as well as to obtain methylpluviatolide derivatives, which are used to manufacture drugs to provide activity at least five times higher than observed for gentian violet and other compounds used heretofore for blood treatment and Chagas' disease prophylaxis.
CN1569862A Anti-tumor platinum (II) complex The invention discloses a group of platinum (II) coordinated complex having effective anticancer activity, which is represented by the structural formula (1) disclosed in the specification, wherein R groups are the same, which are hydrogen atoms or C1-5 alkyl, the cyclohexane diamine is 1,2-trans-cyclohexane diamine, R3 and R4 in formula (3) can be identical or different, which are hydrogen atom or C1-5 alkyl, or can connect with a carbon atom to form a cycloalkyl.
US7423049 e.g., 2-(5-fluoro-2-tolyl)-4-(4-aminocarbonylpiperazinylmethyl)-6-[a-aminocarbonyl-2,6-dichlorobenzyl]pyridine; mitogen-activated protein kinase inhibitor; antiinflammatory agent, autoimmune diseases The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
US20050089933 Compositions and methods for surrogate antibody modulation of an immune response and transport Methods and compositions for the modulation of an immune response are provided. Compositions comprise a bi-functional surrogate antibody molecule that interacts with a ligand of interest, wherein the bi-functional surrogate antibody further has attached thereto an immunomodulatory agent and/or a transporting agent. The compositions of the invention find use in a method for delivering an immunomodulatory agent to a ligand of interest. Further provided are methods for modulating an immune response in a subject against a ligand of interest. The method comprises administering a therapeutically effective amount of a bi-functional surrogate antibody of the invention. The methods of the invention also find use in improving the clinical outcome of a subject in need of a modulation in the immune response. Methods are further provided for the treatment or prevention of a variety of conditions and/or disorders including cancer, autoimmune diseases, allergies, prions, and various diseases or conditions of bacterial, parasitic, yeast or viral etiology.
CN102127067A 2-(6-aminobenzothiazole-2-mercapto)-acetamide derivatives and preparation method and applications thereof The invention belongs to the technical field of the chemical medicine and particularly relates to 2-(6-aminobenzothiazole-2-mercapto)-acetamide derivatives and a preparation method and applications thereof. The first technical problem solved by the invention is to provide a kind of new compounds which are 2-(6-aminobenzothiazole-2-mercapto)-acetamide derivatives shown in the formula I. The 2-(6-aminobenzothiazole-2-mercapto)-acetamide derivatives can be obtained on the basis of a great amount of screenings and the derivatives have antitumor activities; and the invention provides a new option for the development and application of the antitumor drug.
WO2009019607A4 Beta adrenergic receptor ligand derivatives for modulating apoptosis The present invention relates to the new therapeutic uses of beta-3 adrenergic receptor agonist derivatives in particular to inhibit apoptosis and treat and/or prevent apoptosis-related diseases and disorders.
WO2014020480A3 Compositions and methods for the treatment migraine and neurologic diseases The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of migraine and neurologic diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, migraine, Post Herpetic Neuralgia, Acute and Chronic Pain, Alzheimer's disease, Creutzfeld Disease, familial amyloid polyneuropathy, parkinson's disease, fibromyalgia syndrome.
CN102188431A Doxazosin mesylate sustained-release tablets and preparation method thereof The invention relates to doxazosin mesylate sustained-release tablets and a preparation method thereof. The doxazosin mesylate sustained-release tablets comprise tablet cores and sustained-release coatings, wherein the tablet cores contain a hydrophilic gel skeleton material which accounts for 15%-30% of the weight of the tablet cores, and the weight of the sustained-release coatings is 2.0%-5.0% of the weight of the tablet cores. The doxazosin mesylate can be well controlled to release by the doxazosin mesylate sustained-release tablets obtained by the invention, and a drug-release curve similar to that of commercial Cardure XL can be obtained, so that the blood concentration can achieve and keep in a therapeutic concentration range, thereby improving the safety and effectiveness of medication and the compliance of patients.
EP2368876A1 Derivatives of aminoindanes, their preparation and their application in therapeutics The instant invention relates to derivatives of formula (I) and their application in therapeutics.
US20070270339 Use of GPCR54 Ligands for the Treatment of Infertility The present invention is directed to methods and compositions for the treatment of infertility.
CN103340940A Tibetan medicament for treating constipation and preparation method thereof The invention discloses a tibetan medicament for treating constipation and a preparation method thereof. The tibetan medicament consists of active components or active components and pharmaceutically acceptable auxiliaries, wherein the active components are prepared from whim, purpurea halitium, cassiae fructus, tronae and rheum officinale in a certain weight ratio. The tibetan medicament can be produced into an arbitrary common internal preparation, has the functions of clearing heat accumulation, and breaking stasis and eliminating mass, and can be used for treating gastrointestinal accumulated masses, constipation, belch and abdominal pain, gastrointestinal function degradation and other symptoms. The tibetan medicament can be used in constipation with remarkably reduced defection times caused by internal heat and qi depression (every 2-3 days or even longer period per time), irregular constipation, hard excrement and the like.
WO2006081665A1 Purine nucleoside analogs The present invention is directed to purine nucleoside analogs of the general Formula (I), or tautomers thereof, physiologically acceptable salts, solvents and physiologically functional derivatives thereof, and pharmaceutical compositions comprising such compounds, salts and derivatives, which are useful as anti-bacterial and anti-protozoan agents. The invention is also directed to methods for treating a bacterial or protozoan infection in a mammal and use of the compounds for inhibiting the growth of a bacteria or protozoa.
US20110027277 Predictive marker for topoisomerase i inhibitors The present invention generally relates to the fields of cancer therapy and cancer prevention. More particularly, the present invention generally relates to a diagnostic marker for predicting the efficacy of topoisomerase I (topo I) inhibitors in the treatment of cancers. More specifically, the present invention relates to methods, machines, computer systems, computable readable media and kits which can be used to identify and determine the effectiveness of topoisomerase I (topo I) inhibitors in the treatment of cancers, and in some embodiments, the level of sensitivity or resistance of a tumor cell to a topoisomerase I inhibitor, such as camptothecin (CPT), or CTP analogues such as topotecan and irinotecan and derivatives thereof. More specifically, the present invention related to methods, machines, computer systems, computable readable media and kits which can be used to determine the presence of phosphorylation of topoisomerase I polypeptide, in some embodiments phosphorylation at residue serine 10 (S10) of a topoisomerase I polypeptide, wherein the presence of phosphorylation, in particular the phosphorylation at serine 10 of a topoI polypeptide indicates a cancer is likely to be unresponsive to a topo I inhibitor, whereas the absence of phosphorylation, in particular, the absence of phosphorylation at residue serine 10 (S10) identifies a cancer is likely to be responsive to a topo I inhibitor. Other aspect of the present invention relate to phospho-serine 10 topoisomerase I antibodies and other protein binding moieties, and uses thereof.
WO2013163545A1 Use of n-acetylcysteine amide in the treatment of disease and injury This disclosure describes methods of use for N-acetylcysteine amide for the treatment of various disorders
EP2020232A1 N-(1-thiazolyl)-amide derivatives for the treatment of obesity, diabetes and cardiovascular diseases The invention relates to the use of a compound of formula (I) : its pharmaceutically acceptable salts, prodrugs and/or solvates, in the preparation of a medicinal product for the treatment of a disease presenting altered adiponectin levels or in which it is necessary to alter the adiponectin protein levels.
CA2417709C Compositions and dosage forms for application in the oral cavity in the treatment of mykoses A solid dosage form for application in the oral cavity, comprising a poorly bioavailable pharmaceutical active ingredient dispersed in a pharmaceutically acceptable matrix.
US20110191868 Methods for identification and use of agents targeting cancer stem cells The invention relates to methods for identifying compounds and compositions that target cancer stem cells. In some aspects, the invention relates to treatment methods that use compounds and compositions that specifically target cancer stem cells for inhibiting the growth and/or survival of cancer stem cells in a subject in need thereof. Other aspects of the invention relate to the use of cancer stem cell biomarkers in the selection of a treatment for inhibiting the growth and/or survival of cancer stem cells in a subject in need thereof.
WO2008048194A1 Use of the protein kinase c inhibitor tamoxifen for the treatment of bipolar disorder Bipolar subjects with manic/mixed episode were randomly assigned to receive either tamoxifen (80mg/day) or identical placebo tablets in 1:1 ratio for three weeks. At the end of three weeks of trial tamoxifen treatment has been shown to have strong anti-manic properties. Protein kinase C inhibition seems to be one of the direct targets of lithium and valproate, The existing effective treatments in bipolar disorder/mania. These findings may lead to delineation of the underlying pathophysiology of bipolar disorder and development of novel therapeutics.
WO2009157801A1 Method for injecting an anesthetic into tissues The aim of the invention is to increase the efficiency of a local anaesthetic injection by monitoring the pressure of injection of local anaesthetic solutions into tissues taking in consideration the content vasoconstrictors in said solutions. The technical result is achieved by the fact that the local anaesthetic solution is injected into the tissues under a pressure ranging from 0.7 to 1.6 atm.
CA2362515C Utilization of material containing docosapentaenoic acid A novel technique for relieving arachidonic acid deficient conditions and maintaining a good fatty acid balance in vivo. Utilizaiton of a DPA-containing material for relieving arachidonic acid deficient conditions and maintaining a good fatty acid balance in vivo; and compositions for relieving arachidonic acid deficient conditions and maintaining a good fatty acid balance in vivo which contain a DPA-containing material in an amount efficacious in relieving arachidonic acid deficient conditions and maintaining a good fatty acid balance in vivo per unit dose.
CN101084905B Application of ganoderic acid Me in tumoral growth or propagation inhibitor The invention provides the uses of ganoderic acid T and ganoderic acid me in preparation of agents for inhibiting the growth and proliferation of tumor cells. In vitro and in vivo studies have shown that ganoderic acid T and ganoderic acid Me have significant effect of inhibiting the growth and proliferation of human tumor cells while have less toxicity on normal cells. It has good application prospect.
CN103417536A Applications of harmol in preparation of antitumor drugs The invention belongs to the chemical field and the medicine field, relates to and provides applications of harmol in preparation of antitumor drugs, and provides corresponding antitumor drug compositions. The invention also provides a method for inhibition of in vitro tumor cell proliferation. In the method, harmol is added in nutrient solutions of tumor cells. The tumor cells comprise liver cancer cells, stomach cells or leukemia cells. Harmol belongs to a natural product, and has minimal toxic and side effects, high bioavailability, stable properties and clinical use value. The low molecular weight compound can be developed as a new antitumor drug or an auxiliary component thereof, has obvious tumor suppression effects, is environmentally friendly, and provides a new way and method for treating and curing tumors.
WO2006106889A1 Methods of producing sodium alginate-containing tablet and tablets obtained by the production methods [PROBLEMS] To provide a tablet containing a dietary fiber at a high ratio, a dietary fiber tablet containing an essential oil and a method of producing these tablets. [MEANS FOR SOLVING PROBLEMS] A method of producing a tablet containing sodium alginate which comprises tabletting a sodium alginate powder; a method of producing a tablet containing sodium alginate characterized by comprising tabletting a sodium alginate powder and impregnating the obtained tablet with an essential oil; and sodium alginate-containing tablets produced by these production methods. Since sodium alginate can be directly tabletted by compressing a powder, a tablet consisting of sodium alginate alone can be prepared. Thus, a tablet having a large dietary fiber content per unit amount can be obtained. Compared with other tabletting methods, moreover, the above method is advantageous in employing a smaller number of steps and not requiring a high temperature. Furthermore, the tablet thus obtained is highly compatible with an essential oil and thus the essential oil is carried by the tablet in a stable state while showing little oil oozing.
WO2011064508A1 Use of a dipyridyl compound for treating rosacea The present invention relates to a compound with the following formula (I), or any of the pharmaceutically acceptable salts thereof, to be used in the treatment of rosacea.
EP1844767A2 Epoxide hydrolase complexes and methods therewith Biologically stable inhibitors of soluble epoxide hydrolases are provided. The inhibitors can be used, for example, to selectively inhibit epoxide hydrolase in therapeutic applications such as treating inflammation, for use in affinity separations of the epoxide hydrolases, and in agricultural applications. A preferred class of compounds for practising the invention have the structure shown by Formula I wherein X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R1-R4 is hydrogen, R2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R1 and R3 are each independently a substituted or unsubstituted alkyl, haloalkyl, cycloakyl, aryl, acyl, or heterocyclic, or being a metabolite or degradation product thereof.
CN101224248B Medicine for treating heart, lung, liver, kidney hydrocele and preparing method thereof The invention discloses a drug used for curing heart hydrops, wet lung, hydrohepatosis and uronephrosis, which comprises the preparations made from the following crude drugs by weight portion: 120-180 portions of caulis akebiae, 40-80 portions of climbing fern spore and 12-14 portions of oval kumquat root. The crude drugs are crushed according to the weight proportion, mixed and then loaded in a cloth bag which is then soaked in liquor with 30-40 degrees for 20-30 days at normal temperature and then filtered, thus the drug of the invention is obtained; the dosage of the liquor is 100 times the total weight of the crude drugs. The invention is characterized by short course of treatment, quick effect and high effective rate, good effect on relieving a cough and no toxic side effect.
US20090155307 Immunostimulatory nucleic acid oil-in-water formulations and related methods of use The invention involves methods and compositions of an immunostimulatory nucleic acid in oil-in-water emulsions for topical delivery. The compositions can be used to stimulate immune responses, particularly useful in the prevention and/or treatment of infectious disease and cancer.
CN101269020A Glycyrrhizic acid sustained-release dropping pills and preparation method thereof The invention discloses a medicine composition used for curing hepatitis. The invention aims at making up the deficiency of the oral pharmaceutical preparation used for curing hepatitis and provides an oral preparation glycyrrhizin sustained-release pill which has the advantages of high bioavailability, rapid effect, high medication content, controllable medicine release, few times needed by the patient to take the medicine, convenient medicine taking, low price and no pollution in the production. The glycyrrhizin sustained-release pill related by the invention takes mono-glycyrrhizic acid sylvite or mono-ammonium glycyrrhizinate that is active ingredient of glycyrrhiza uralensis fiseh as the raw material, and can be prepared together with medicated carrier that takes hydrophilic framework material and hydrophobic framework material as stroma.
CN103239520A Moslemic ointment for treating osteoarthritis and preparation method of moslemic ointment The invention related to a moslemic ointment for treating osteoarthritis. The ointment is an unguent prepared with angelica sinensis, himalayan teasel root, olibanum, myrrh, caulis spatholobi, ligusticum wallichii, lycopodium clavatum, radix clematidis, eucommia ulmoides and borneol serving as raw materials. According to the moslemic ointment, the main raw materials are aromatic medicines having the effects of activating blood circulation to dissipate stasis and softening hardness to dissipate stagnation and the auxiliary raw materials are the medicines with effects of invigorating liver and kidney, warming meridians to dissipate cold, activating meridians to stop pain and the like, thereby realizing the effects of activating blood circulation to dissipate stasis, relaxing muscles and tendons, dispelling wind and eliminating dampness, softening bony spur, relieving swelling and pain and strengthening tendons and bones; simultaneously, the ointment is prepared into an ointment preparation; and vegetable oil and bee wax which have the effects of diminishing inflammation and moistening skin, activating blood circulation to dissipate stasis and relieving swelling and pain, are adopted as the substrates, therefore, the ointment is gentle to the skin, ensures the continuous effect and therapeutic effect of the aromatic medicines, and has the advantages of low cost, short course of the treatment, high efficiency, great therapeutic effect and no toxic or side effects.
EP2453902A1 Mixture of non-digestible oligosaccharides for stimulating the immune system Nutritional compositions with fucosyllactose and betagalactooligosaccharides for use in stimulation of the immune system. The composition is suitable for infants.
CN102716127A External use pharmaceutical preparation for curing mycotic infection The invention discloses an external use pharmaceutical preparationfor curing mycotic infection, which is composed of active ingredients and medical auxiliary materials, wherein the active ingredients are terbinafine hydrochloride and cetylpyridinium chloride, and preferably, the weight ratio of the terbinafine hydrochloride and the cetylpyridinium chloride is 1-5 to 1. The medicine provided by the invention has better fungus killing effect, is low in rate of relapse, and is anti-inflammatory and antipruritic.
US20090082471 Deuterium-enriched fingolimod The present application describes deuterium-enriched fingolimod, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN103044483A Triphenyltin (IV) coordination compound and preparation method and application thereof The invention discloses a triphenyltin (IV) coordination compound which has the following structural formula shown in the specification, wherein Ph represents phenyl. A preparation method comprises the following steps of: adding 2.0mmol of o-vanillin m-aminobenzoic acid Schiff alkali, 1.0-1.2mmol of triphenyltin oxide and 20-30mL of methanol into a reaction container; stirring for backflow for 6-8 hours at 60-80 DEG C; performing rotary evaporation to obtain an orange solid; and recrystallizing with diethyl ether-petroleum ether to obtain an orange transparent crystal which is an organic tin coordination compound, wherein the volume ratio of diethyl ether to petroleum ether is (1:1)-(2:1). Compared with common platinum anti-cancer compound, the organic tin coordination compound disclosed by the invention has the characteristics of high anti-cancer activity, good lipid solubility, low cost, simple preparation method and the like, and provides a new means of developing an anti-cancer drug.
WO2006115137A1 2-aminobenzimidazole derivative and use of the same for medical purposes Disclosed is a 2-aminobenzimidazole derivative which is effective for a disease cause by abnormal serum uric acid level. A 2-aminobenzimidazole derivative represented by the general formula (I) or a prodrug thereof or a pharmacologically acceptable salt of the compound or prodrug or the like; or a pharmaceutical composition comprising the compound, prodrug or salt as the active ingredient; or the like. (I) wherein R1 represents a halogen atom or the like; m is an integer of 0 to 2; n is an integer of 1 to 2; R2 represents OH or the like; R3 and R4 dependently represent H or OH; the ring Q represents a heterocyclic ring or a bicyclic hydrocarbon group; R5 and R6 independently represent a cyano group, -AH, -A-D-E-G or the like (where A represents a single bond, O, S, NR8 or the like; D represents an alkylene or alkenylene group which may be substituted or the like; E represents a single bond, O, S, NR9 (where R8 and R9 independently represent H or an alkyl group which may be substituted), a (hetero)cycloalkylene or (hetero)arylene group which may be substituted or the like; G represents H, an alkyl or alkenyl group which may be substituted or the like); R7 represents H, a halogen atom, a (hetero)aryl group which may be substituted or the like.
US20120149698 Nouvel compounds The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
CN103505626A Antipyretic medicine The invention relates to an antipyretic medicine which comprises the following raw materials by weight: 30g plaster stone, 10g cortex lycii radicis, 3g indico naturalis, 15g lonicera japonica, 10g weeping forsythia, 10g radix rehmanniae, 10g chrysanthemum, 10g radix ophiopogonis, 6g radix scrophulariae and 5g mint (taking at night). A taking method of the medicine comprises the steps that the plaster stone, the cortex lycii radicis, the indico naturalis, the lonicera japonica, the weeping forsythia, the radix rehmanniae, the chrysanthemum, the radix ophiopogonis and the radix scrophulariae are mixed and put into a medicine pan; 1000g clear water is added for soaking for 30min; boiling is performed by a big fire; slow decoction is performed by a slow fire until 450g water is remained; 5g mint is added and decocted for 2min; dregs are removed; a filtrate is obtained; and a dose is taken every day after the filtrate is at a room temperature. The medicine is taken 1h after a dinner every day, and a patient can be cured after taking 2-4 doses. By clinical use demonstration, the medicine has a good effect on treating a fever and unknown heat energy; the medicine has the advantages that the medicine is high in effectiveness and low in cost, and the raw materials are easy to obtain and easy to prepare; the medicine has no toxic or side effects; and the safety of medicine use of the patient is ensured.
WO2013084060A1 Quaternized buprenorphine analogs The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R1a, R2, R8, R3a, R3b, G, X, Z, Y, and A ® are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
CN102813638A Preparation method of dexketoprofen trometamol double-layer sustained-release tablets The invention relates to dexketoprofen trometamol double-layer sustained-release tablets and a preparation method thereof. The tablets are characterized in that the tablets are double-layer tablets obtained by compacting a fast-release layer and a sustained-release layer. The fast-release layer is mainly composed of dexketoprofen trometamol, a disintegrating agent, a diluent agent, an adhesive, and a lubricant. The sustained-release layer is mainly composed of dexketoprofen trometamol, a sustained-release material, a diluent agent, an adhesive, and a lubricant. An effective dosage of dexketoprofen trometamol is 10mg-120mg. A main medicine content ratio of the fast-release layer to the sustained-release layer is 1:(1-5). The invention also provides a preparation method of the dexketoprofen trometamol double-layer sustained-release tablets, and a release-degree testing method of the tablets. With the release of the fast-release part of the dexketoprofen trometamol double-layer sustained-release tablets provided by the invention, an effective blood concentration of the medicine can be reached fast. The sustained-release part is released slowly for maintaining a stable and uniform effective blood concentration. Therefore, medication times can be reduced, patient compliance can be improved, the treatment effect is stable, and toxic and side effects are low.
CN101890013A Pitavastatin calcium composition stabilized by using alkaline reagent and preparation method thereof The invention relates to a medicinal composition, in particular to a pitavastatin calcium composition stabilized by using an alkaline reagent and a preparation method thereof. The pitavastatin calcium composition is characterized in that: the alkaline reagent is magnesium oxide, the pH of the aqueous solution or the suspension of the magnesium oxide is more than 9 and less than 12, and the alkaline reagent can remarkably improve the stability of the pitavastatin calcium composition. The pitavastatin calcium composition is suitable for long-term storage and has good clinical effect. The preparation method for the pitavastatin calcium composition is simple, convenient to operate and suitable for industrialized production.
US20130064913 Anti-inflammatory botanical products for the treatment of metabolic syndrome and diabetes Disclosed are botanically based compositions and methods useful for the treatment of metabolic syndrome and diabetes type 2. Compositions, kits, and methods are additionally disclosed for means to augment the activity of identified glucose and insulin regulating drugs.
WO2006010598A1 Non-glycosidic and non-peptidic select inhibitors, and the use thereof The invention relates to a category of non-glycosidic and non-peptidic select inhibitors of general formula (1), with a low molecular weight, and to a method for the production thereof. Said category is a category of non-toxic select inhibitors having an anti-inflammatory effect in vivo, which does not have the disadvantages of the glycosidic inhibitor complexes, and is potent in vitro, as the known active ingredient bimosiamose. The invention also relates to medicaments containing said compounds and to the use thereof for the treatment of diseases.
WO2010054968A1 Quinazoline derivatives as nk3 receptor antagonists The present invention relates to a compounds of formula I wherein R1 is hydroxy or NR'R"; R' and R" are independently from each other hydrogen, lower alkyl, cycloalkyl, or may form together with the N-atom to which they are attached a heteroalkyl ring; R2 is hydrogen, lower alkyl, lower alkoxy, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano or S(O)2-Iower alkyl; R3 is lower alkyl, -(CH2)m-aryl, optionally substituted by halogen, or is -(CH2)m-cycloalkyl; R4 and R5 are independently from each other hydrogen or lower alkyl substituted by halogen, or are -(CR2)m-aryl or -(CR2)m-heteroaryl, wherein the rings may be substituted by one or more substituents, selected from halogen, lower alkyl, lower alkyl substituted by halogen, cyano, hydroxy, NR'R" or by lower alkoxy substituted by halogen, or are -(CR2)m-cycloalkyl, optionally substituted by hydroxy or by aryl, or are a heteroalkyl ring, optionally substituted by =O or -(CR2)m-aryl, or R4 and R5 are together with the N-atom to which they are attached a heterocyclic ring system, optionally substituted by lower alkyl, aryl or halogen-substituted aryl, and R may be independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; m is 0, 1 or 2; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
WO2014066243A1 Solid forms of {s-3-(4-amino-1-oxo-isoindolin-2yl)(piperidine-3,4,4,5,5-d5)-2,6-dione} The invention in one embodiment is directed to solid forms of { S-3-(4- Amino- 1 -oxo- isoindolin-2-yl)(piperidine-3,4,4,5,5-d5)-2,6-dione}, including an anhydrous crystalline form, two hydrates, and an amorphous form. The invention in one embodiment is directed to methods of preparation of the solid forms.
EP1379523B1 1,2,3,4-tetrahydroisoquinolines derivatives as urotensin ii receptor antagonists The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists especially urotensin II antagonists.
EP2123271B1 Drug for treatment of influenza Disclosed is a drug for treatment or prevention of H5N1 influenza. Specifically disclosed is a drug for treatment or prevention of H5N1 influenza, which contains a compound represented by the general formula (I) below as an active ingredient. (I) (In the formula, R1 and R2 represent an H or an alkanoyl; X represents a halogen atom, an OH, an alkoxy or an alkanoyloxy; and R3 represents an H or an alkyl. In this connection, the case wherein R1 and R2 are respectively an H, X is an OH and R3 is an H is excluded.)
CN102367257A Single-crystal crystal forms of clopidogrel hydrochloride and preparation method and application thereof The invention relates to single-crystal crystal forms of clopidogrel hydrochloride and a preparation method and application thereof. The single-crystal crystal form is the monoclinic system, wherein the crystal axes are as follows: a = 9.2985 (5), b = 8.8930 (4) and c = 21.2663 (15); and the crystal plane angles are as follows: alpha = 90 degree, beta = 101.575 (5) degree and gamma = 90 degree. In addition, the invention also relates to pharmaceutical compositions with the single-crystal crystal form, wherein the pharmaceutical compositions are used to prevent and treat atherothrombosis.
CN1903192A Antiviral medicine, prepn. method and application thereof An antiviral medicine is prepare from C-21 steroid and medicinal carrier. It can selectively suppress the alphavirus-like viruses and prevent and treating their associated diseases. Its preparing process is also disclosed.
EP2370405A1 Triple reuptake inhibitors and methods of their use Provided herein are bicyclic compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders. Compounds provided herein inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations containing the compounds are also provided.
WO2005094896A3 Targeted serotonin reuptake inhibitors A serotonin reuptake inhibitor which can be used in the treatment of depression and which has a decreased occurrence of unwanted side effects. The serotonin reuptake inhibitors are bi-functional organic molecules which combine serotonin transporter reuptake inhibition with serotonin (5-HT,such as 5-HT2A) receptor antagonism in one molecular entity. The serotonin-selective reuptake inhibitor (SSRI) homologue portion of the molecule shows an affinity to the serotonin reuptake transporter (SERT) and has antidepressant properties. The piperazine or piperidine portion of the molecule demonstrates an affinity to 5-HT receptors and restores the undesired side effects of SSRIs.
EP1255724B1 Substituted norbornylamino derivatives, method for the production thereof, use thereof as a medicament or a diagnostic reagent and medicaments containing said compounds The invention relates to substituted norbornylamino derivatives containing exo-configured nitrogen and an endo-annellated pentacyclic ring of formula (I) and exo-configured nitrogen and an exo-annellated pentacyclic ring of formula (Ia), wherein R1, R2 R3, R4, R5, A, B, S1 and S2 have the meanings cited in the claims. Said derivatives are especially suitable as anti-hypertensive agents for reducing or preventing ischaemia-induced damage, as medicaments for use in surgical procedures for treating ischaemias of the nervous system, of a cerebrovascular accident and of a cerebral oedema. The derivatives are also suitable for treating shock, an impaired respiratory impulse, snoring, or for use as a laxative, as an agent against ectoparasites, in the prophylaxis of gall stones, as an anti-atherosclerotic agent, as an agent for treating late complications of diabetes, or for treating cancerous illnesses, fibrotic disorders, endothelial dysfunction and organ hypertrophies and hyperplasias. Said derivatives act as inhibitors of the cellular sodium-proton-antiporter. They also influence serum lipoproteins and can thus be used in the prophylaxis and reversal of atherosclerotic changes.
US20080103094 Targeted delivery of drugs for the treatment of viral infections Conjugates of transferrin or transcobalamin with anti-viral agents are useful in the treatment of viral infections. Suitable anti-viral agents include apoptosis inducing compounds, compounds which inhibit the replication of the virus, a cytotoxic antibiotic, an alkylating agent, a plant toxin, and a bacterial mutant toxin. Transferrin or transcobalamin is preferably coupled to the anti-viral agent by means of glutaraldehyde.
EP1517898A1 Arylcarbonylpiperazines and heteroarylcarbonylpiperazines and the use thereof for treating benign and malignant tumour diseases The invention relates to novel arylcarboxamides and heteroarylcarboxamides of general formula (I), to the production thereof, and to the use of the same as pharmaceuticals, especially for treating tumours.
WO2011123027A1 Improved treatment of renal cell carcinoma Methods for treating renal cancer by administration of certain 3,3',4,4'-tetrahydroxy-2,2'- bipyridine-N,N'-dioxide compounds, especially 3,3',4,4'-tetrahydroxy-2,2'-bipyridine-N,N'- dioxide (Orellanine), conjugated to an alpha-emitting radionuclide (e.g. Astatine-211) to increase the efficacy of the formulation and/or a large molecule (e.g. a oligomer/polymer such as a PEG or a polysaccharide such as a dextran or a Ficoll®) to reduce the filtration and consequently the renal exposure. Particular administration protocols and dosing regimens, as well as pharmaceutical compositions suitable for use in the treatment methods can be used.
WO2007009392A1 The use of chlorogenic acid in the manufacturing medicaments for treating and/or preventing hepatic injury The use of chlorogenic acid in the manufacture of medicaments for treating and/or preventing hepatic injury . The pharmaceutical composition possessing the corresponding use . It is proved by pharmacodynamic test that chlorogenic acid could treat and./or prevent hepatic injury . Chlorogenic acid is derived from nature plant , has the lower toxicity and can improve the whole function of body , therefore , it provides a new option for clinic .
WO2014164969A1 Treatment of cataplexy The present invention relates to a method of treating cataplexy in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of certain carbamate compounds.
CN103550197A Application of guluronic acid oligosaccharide The invention discloses the application of guluronic acid oligosaccharide. The guluronic acid oligosaccharide is used for preparing a nitric oxide generation accelerant. Through research, the guluronic acid oligosaccharide can activate macrophages to express iNOS mRNA and protein, so as to accelerate the generation of NO. Therefore, the guluronic acid oligosaccharide can serve as the nitric oxide generation accelerant.
US20110318406 Lecithin carrier vesicles and methods of making the same A hydrated lecithin carrier vesicle composition includes a lecithin-derived membrane-forming lipid vesicle in conditioned water for incorporation of an active ingredient to form a dispersed composition. A method of making the hydrated lecithin carrier vesicle includes using lecithin having not more than about 80% w/w phosphatidylcholine in the presence of conditioned water.
WO2006083434A1 Use of arachidonic acid and its derivatives for increasing skeletal muscle mass This invention discloses a method of orally administering arachidonic acid and its derivatives for the purpose of increasing the serum level of the prostaglandin PGF2alpha and subsequently the level of retained skeletal muscle mass.
WO2008020206A3 Fused thiophene derivatives as mek inhibitors Compounds of formula (I), or a pharmaceutically acceptable salts or solvates thereof : wherein -X- represents a group of formula (a), (b), (c), (d), (e), (f) or (g) : Being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive
US20080009512 Tetrahydroquinolones and Aza-Analogues Thereof for Use as Dpp-IV Inhibitors in the Treatment of Diabetes Compound of formula (I) or a pharmaceutically-acceptable salt thereof, formula (I) wherein Ar is optionally substituted phenyl; R1 is selected from: formula a) or b) (wherein is a single or double bond); R5, R6, R7 and R8 are for or alkyl; R4 is selected from hydrogen, (3-4C)cycloalkyl and optionally substituted (1-4C)alkyl; R10 is for example selected from hydrogen, (1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, hydroxy(1-4C)alkyl, (1-4C)alkoxy, aryl(1-4C)alkyl; Y is carbon and Ring A is optionally substituted phenylene; or each Y may independently be carbon or nitrogen and Ring A is optionally substituted 5- or 6-membered, heteroarylene ring; R11 is selected from hydrogen and optionally substituted phenyl; p is independently at each occurrence 0, 1 or 2; are described. Processes for making such compounds and their use as DPP-IV inhibitors in the treatment of diabetes are also described.
WO2011035343A3 Phentermine liquid dosage form The invention provides a pharmaceutical composition liquid dosage form of Phentermine, said dosage form including a liquid carrier and suspended or dissolved therein one or more pharmaceutically active ingredient selected from Phentermine, salts and bases thereof, and a pro-drug thereof. The invention extends to a method of administering Phentermine to an obese patient in need thereof and for appetite suppression or related conditions.
CN102985093A Agent for suppressing the formation of abnormal skin cells caused by exposure to light An object of the present invention is to provide an agent for suppressing the formation of skin cells induced by exposure to light such as ultraviolet light. The object is achieved by using a purine nucleic acid for suppressing the formation of abnormal skin cells caused by exposure to light.
CN101422466A Use of cucurbitacin in preparing medicine for treating cancer The invention relates to the new application of cucurbitacin in preparing a medicament for curing cancers. The invention relates to the application of the cucurbitacin in preparing a medicametn for curing liver cancer. Test proves that the cucurbitacin has remarkable inhibition or killing effects on various cancers such as liver cancer, lung cancer, gastric cancer, laryngocarcinoma, leukemia, and the like. The action intensity of the cucurbitacin is relevant to a preparation formulation, a medication approach and dosage.
CA2377614C Anesthetic composition for intravenous injection comprising propofol The present invention relates to an anesthetic composition for intravenous injection, characterized in that it contains propofol (2,6-diisopropylphenol) and a poloxamer as the surfactant. The composition of the present invention can optionally contain at least one co-surfactant selected from the group consisting of Solutol HS 15, egg lecithin, Labrasol, polyoxy 10- oleyl- ether, tween, ethanol and polyethylene glycol. Since the composition of the present invention is prepared in the form of a microemulsion having a particle size of 100nm and below, it has a superior technical effect that it is thermodynamically stable, can be aseptically filtered to prevent the microorganisms contamination, and further, can be readily prepared and can minimize side effects including embolism and hypereipidemia, etc.
CN102516113A A series of diphenyl oxide derivatives and use of diphenyl oxide derivatives in preparation of anti-tuberculosis drugs The present invention relates to a series of diphenyl oxide derivatives and a use of the diphenyl oxide derivatives in preparation of anti-tuberculosis drugs, and belongs to the field of chemical medicine. Specifically the present invention relates to a use of a compound represented by a formula (I), wherein Ar1 is a substituted benzene ring, n is an integer of 0-3, R1 is a substituted benzene ring Ar2 or a substituted heterocyclic Het. The test results show that the compound represented by the formula (I) provides good in vitro inhibition activity for tubercle bacillus H37Rv, provides a good treatment effect for in vivo BCG infection mice model, and provides a new selection for preparation of the anti-tuberculosis drugs.
EP1807407B1 Aromatic amides as inhibitors of c-fms kinase The invention relates to compounds of Formula (I), wherein A, X, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula (I), are also provided.
US20100081648 Methods for Characterizing and Treating Cognitive Impairment In Aging and Disease This invention provides methods for identifying genes associated with cognitive impairment and for identifying compounds useful in the treatment of cognitive impairment. The methods can in particular be used to identify genes associated with, and compounds useful in treating, cognitive impairment in aging.
CN103027963A Health care composition for relaxing bowels and improving organism immunity and preparation method The invention discloses a health care composition, an oral liquid and a health care product for relaxing bowels and improving organism immunity, and a preparation method of the health care composition, the oral liquid and the health care product. The composition is prepared by mixing extractives extracted from semen cassiae, polygonum multiflorum and gynostemma pentaphyllum by enthanol with fructooligosaccharide; a sugar aspartame sweetener and a citric acid additive are added to the prepared health care composition and filled to be prepared into the oral liquid; corresponding pharmaceutical necessities can also be added to be prepared into a capsule or troche, the health care composition, the oral liquid and the health care product have functions of relaxing the bowels and improving the organism immunity, and have no adverse reactions to body health, and the preparation method of the health care composition, the oral liquid and the health care product is simple; no additional cost exists; and the method can be widely used for industrial production.
US7247636 Phenolic guanidine sodium channel blockers The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using these sodium channel blockers.
US7087244 Thermogelling oligopeptide polymers Disclosed is a thermogelling biodegradable aqueous polymer solution useful in providing a bioactive agent delivery system. A thermogelling biodegradable aqueous polymer solution may comprise a biocompatible block and a biodegradable polypeptide block, where the blocks are linked to form a polymer of a general structure comprising the formula of CnDm, wherein n is equal to or greater than 1, m is equal to or greater than 1, C is a biodegradable polypeptide block, and D is a biocompatible soluble polymer having a chain length such that if D is not biodegradable, D may be eliminated through a glomeruli filtration system.
US20080139633 Estrogen receptor modulators; neurodegenerative disorders; cognitive enhancement The present invention is directed to a hydrate crystal form (designated as Form F herein) of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol, an estrogenic receptor modulator useful in the treatment of, for example, diseases related to abnormal levels of estrogen.
CN1846710A Vagina cleaning agent The vagina cleaning agent as one kind of sterilizing health care article has high sterilizing effect, less stimulation, no influence on environment balance inside vagina, nourishing effect and high stability. It consists of iodine, co-solvent potassium iodide, sodium iodide or ammonium iodide, carrier alkylphenol ethoxylate, pH regulator amino acid or its salt and water as solvent in certain weight proportion.
CN102600068A Stable ready-to-use paracetamol preparation capable of being injected The invention relates to stable paracetamol water solution used for intravenous injection. The solution contains at least one soluble compound used for stabilizing paracetamol solution and the soluble compound is selected from hydroxyalkyl-cyclodextrion and at least one stable compound, wherein the concentration of the stable compound is between 0.001% m/v and 20%m/v, and the stable compound is EDTA (ethylene diamine tetraacetie acid) or monothioglycerol which can be used alone or used in a combined manner.
EP1317188B2 Use of benzophenanthridine alkaloids as feed additives The invention relates to an animal feed, containing conventional feed materials such as cereal or cereal products, maize, proteins and aromatic amino acids, vitamins, mineral aggregates such as salts, phosphates, lime, enzymes and similar and an effective amount of one or several benzophenanthridine alkaloids, or derivatives or synthetic analogues thereof to reduce the enzymatic degradation of the essential aromatic amino acids. The invention further relates to the use of benzophenanthridine alkaloids, derivatives or synthetic analogues thereof and a medicament.
EP1400515B1 Cyclic diamine compound having five-membered cyclic group A compound represented by the following general formula (1): (1) (wherein A represents a single bond, C ≡ C, CONH, or NHCO; W represents carbon or nitrogen; X represents CH, nitrogen, oxygen, or sulfur; Y represents CH, CHR1, nitrogen, oxygen, sulfur, or NR2; Z represents nitrogen, oxygen, sulfur, CH, or NR3; m is 1 or 2; n is a number of 1 to 5; and R1, R2, and R3 each represents hydrogen, lower alkyl, lower alkyl substituted by hydroxy, lower alkyl substituted by lower alkoxy, aryl, lower alkyl substituted by aryl, or lower alkyl substituted by heteroaryl; provided that one or two of W, X, Y, and Z are heteroatoms), an acid addition salt of the compound, or a hydrate of either; and a medicine containing any of these. The compound (1) has inhibitory activity against cell adhesion and cell infiltration. It is useful for allergy, asthma, rheumatism, arteriosclerosis, inflammation, etc.
EP1951048A2 Flavanols and b-type procyanidins and inflammation The invention relates to compositions, and methods of use thereof, containing certain polyphenols such as flavanols, procyanidins and derivatives thereof for treating inflammation and/or inflammation-related or associated disease or condition, and/or for the relief of pain, in a subject sensitive to a selective cyclooxygenase-2 (COX-2) inhibitor and/or a subject sensitive to a COX-nonselective nonsteroidal anti-inflammatory drug (NSAID).
US8173654 Triazolopyridazine compounds The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
WO2011073231A1 3,4,4A,10B-TETRAHYDRO-1H-THIOPYRANO-[4, 3-c] ISOQUINOLINE DERIVATIVES The compounds of formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.
CN102046152A Pharmaceutical composition with bisphosphonate The present invention relates to depot formulations comprising a poorly water soluble salt of a bisphosphonate forming together with one or more biocompatible polymers, to poorly water-soluble salts of such bisphosphonates, to crystalline forms of the free compounds and the salts and to other related aspects, where the compounds are of the Formula (I), where R1 and R2 are as described in the specification. Compounds of the Formula (I) and their forms mentioned in the disclosure are useful for the treatment of bone-related disorders and cancer.
CA2716514A1 Hiv protease inhibitor and cytochrome p450 inhibitor combinations Compositions and methods of treating viral infections are provided. More particularly, compositions including a combina-tion of protease inhibitors and cytochrome p450 enzyme inhibitors are provided. Methods of using the compositions for treatment of diseases or disorders caused by a virus such as HIV infections are also provided.
WO2009000163A1 1β- METHYLCARBAPENEM ANTIBIOTICS,THE PHARMACEUTICAL COMPOSITION AND USE THEREOF Antibiotic 1β-methylcarbapenem compounds of formula(I),pharmaceutically acceptable salts, in vivo hydrolysable esters, isomers, preparations or compositions thereof, or their use in the manufacturing of medicaments which prevent and/or treat infection diseases in mammals including human.
US20100317716 RNA INTERFERENCE MEDIATED INHIBITION OF TNF AND TNF RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) This invention relates to compounds, compositions, and methods useful for modulating tumor necrosis factor and/or tumor necrosis factor receptor gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of tumor necrosis factor and/or tumor necrosis factor receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of tumor necrosis factor and/or tumor necrosis factor receptor genes, (TNF and/or TNF receptor).
US20060210619 Limposomes containing asiaticoside and the uses thereof This invention belongs to the chemical field, which is related to the fields of pharmaceutical preparations and cosmetic, especially to asiaticoside-liposome and its use for preparing pharmaceutical preparations and cosmetic. In this invention, asiaticoside and lipid components are fused by heating or dissolved in organic solvents, then treated with the rotary thin layer evaporation technique, hydrated by adding aqueous solution under shaking to afford lipid dispersing aqueous solution, and then treated by using the technics of sonication, homogeneous emulsification, microjet and extruding filtration to enwrap asiaticoside in the middle of liposomal bilayer membranes to form the hydrophilic asiaticoside-liposome. Asiaticoside-liposome of this invention can enhance the stability, skin penetrability and hydrophilicity of asiaticoside, it can be used for the preparation of cosmetic and pharmaceutical preparations especially skin-penetrated pharmaceutical preparations, and it is more convenient and easy to prepare skin-penetrated pharmaceutical preparations and cosmetic containing asiaticoside.
WO2013064594A1 Gold compounds having alkynyl ligands and therapeutic use thereof The present invention relates, in a first aspect, to novel angiogenesis inhibitors based on gold(I)-alkynyl complexes. More specifically, the present application relates to the use of compounds having a phosphine or carbene group, Au(I), alkynyl and an aromatic optionally bonded to the alkynyl via a linker. These compounds show excellent inhibition of angiogenesis in a person. In addition, for carbene-containing compounds according to the present application, cytotoxic properties have been shown, more particularly for treatment of cancer. The present application further relates to novel pharmaceutical compositions comprising carbene-gold(I)-alkyne complexes, and to novel antirheumatics, angiogenesis inhibitors or cytostatics.
CA2379605C Topical suspension formulations containing ciprofloxacin and dexamethasone Suspension formulations containing dexamethasone and ciprofloxacin are disclosed. The formulations contain a nonionic polymer, a nonionic surfactant and an ionic tonicity agent, but are physically stable and easily re-suspended. The formu-lations are intended for topical application to the eye, ear or nose.
WO2013115636A1 Composition for the treatment and/or prevention of fatty liver disease There is provided at least one method of treating, preventing, ameliorating, reducing or delaying the onset of fatty liver disease (FLD) using tocotrienol or derivative thereof or a mixture thereof.
CN103724296A Aryl substituted piperazine carbonyl derivative as well as preparation method and application thereof The invention discloses aryl substituted piperazine carbonyl derivative as well as a preparation method and application thereof. The aryl substituted piperazine carbonyl derivative is free alkali or salt of a compound adopting a general formula (I) shown in the Specification, wherein the salt is one of hydrochloride, hydrobromide, sulfate, trifluoroacetate, tartrate, lactate or mesylate; Ar independently represents aryl, substituted heterocyclic ring or substituted aryl; R1 independently represents (-O-CH2-) or (-CH=CH-); R2 and R3 can be the same or different, and respectively and independently represents H, halogen, alkyl, halogen substituted alkyl, nitro, amino, nitrile group, hydroxyl, alkoxy, aryl alkoxy, heterocyclic ring alkoxy, aryl, substituted heterocyclic ring or substituted aryl. The aryl substituted piperazine carbonyl derivative can be applied to the preparation of drugs for treating cerebral arterial thrombosis.
US20120157446 Medical use The present invention relates to a method for the treatment of urticaria which comprises administering to a patient in need thereof an effective amount of a compound which is 4-[(4-chlorophenyl)methyl]-2-({(2R)-1-[4-(4-{[3-(hexahydro-1H-azepin-1-yl)propyl]oxy}phenyl)butyl]-2-pyrrolidinyl}methyl)-1(2H)-phthalazinone, or a pharmaceutically acceptable salt thereof.
EP1551370B1 Aggregate with increased deformability, comprising at least three amphipats, for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin The application describes combinations of at least three amphipatic substances forming aggregate suspensions in a polar liquid. Judicious choice of system components, which differ at least 2-times to 10-times in solubility, ensures said aggregates to have extended, unusually adaptable surfaces. This is probably due to simultaneous action on said aggregates of at least two more soluble substances amongst said three system components, at least one of which is an active ingredient and preferably a drug; the third component, alternatively, can take the role of a drug. The application further deals with the use of said combinations in pharmaceutical preparations capable of transporting drugs into the body of warm blood creatures. This is made possible by the drug loading capability of said aggregates with the highly flexible and deformable coating, which renders the resulting drug carriers highly adaptable. The application finally reveals suitable methods and favourable conditions for carrier manufacturing and application. The application also describes novel formulations of nonsteroidal anti-inflammatory drugs (NSAIDs) based on complex aggregates with at least three amphipatic components suspended in a suitable, e.g. pharmaceutically acceptable, polar liquid medium.
US20080269148 Using vector comprising nucleotide sequences which interfere with viral gene expression for prevention and treatment of hepatitis c viral infection; gene expression inhibition The present invention provides double-stranded RNA molecules that mediate RNA interference in target cells, preferably hepatic cells. The invention also provides double-stranded RNA (dsRNA) molecules that are modified to be resistant to nuclease degradation, which inactivates a virus, and more specifically, hepatitis C virus (HCV). The invention also provides a method of using these modified RNA molecules to inactivate virus in mammalian cells and a method of making modified small interfering RNAs (siRNAs) using human Dicer. The invention provides modified RNA molecules that are modified to include a dsRNA or siRNA wherein one or more of the pyrimidines in the RNA molecule are modified to include 2′-Fluorine. The invention also provides dsRNA or siRNA in which all pyrimidines are modified to include a 2′-Fluorine. The invention provides that the 2′-Fluorine dsRNA or siRNA molecule is further modified to include a two base deoxynucleotide “TT” sequence at the 3′end of the molecule.
US20080176948 Topical Anesthetic for Rapid Local Anesthesia and Method of Applying a Topical Anesthetic A topical anesthetic for rapid local anesthesia is provided. The topical anesthetic includes an anesthetic, volatile and non-volatile solvents, and a thickener. In addition, a method is taught for applying the topical anesthetic to the face of a patient without occlusion. The anesthetic is applied topically to an area for injection such that the dermatological procedure (cosmetic injections) can be performed in fifteen minutes.
US20090104256 Methods of Treating Pulmonary Disorders with Liposomal Amikacin Formulations Disclosed herein are methods of treating pulmonary disorders comprising administering to the patient an effective dose of a nebulized liposomal amikacin formulation for at least one treatment cycle, wherein: the treatment cycle comprises an administration period of 15 to 75 days, followed by an off period of 15 to 75 days; and the effective dose comprises 100 to 2500 mg of amikacin daily during the administration period.
US20090317496 Method for Preventing and Treating the Disease Caused by Vascular Damage and the Use Thereof The present invention relates to compositions containing an extract of processed Panax genus plant and saponin compounds isolated therefrom for treat the diseases caused by vascular injury in human or mammal, the method for treating said diseases using thereby and the use thereof. The extract of processed Panax genus plant and saponin compounds isolated therefrom shows suppressive effect on endothelial dysfunction and damage of blood-retinal on HUVEC and retinal vascular endothelial cell. Therefore, it can be used as the therapeutics or functional health food for treating and preventing the diseases caused by vascular injury.
US20100247587 Pigmentation-regulating compounds The present invention relates to compounds of general formula (I): wherein X is selected from the group consisting of O or S and R is a linear or branched, saturated or unsaturated aliphatic group with from 2 to 23 carbon atoms (C2 to C23), or a cyclic group, and which can contain substituents selected from the group consisting of hydroxy, alkoxy, amino, carboxyl, cyano, nitro, alkylsulfonyl or halogen atoms, a method of obtaining them, cosmetic or pharmaceutical compositions containing them and the use thereof for treating, caring for and/or cleaning skin, hair and/or nails, preferably those conditions, disorders or pathologies of the skin, hair and/or nails which require regulating melanogenesis.
WO2013157833A1 Composition including beta-blocker as an active principle for treating or improving obesity, metabolic diseases, and osteopenia The present application discloses a composition including beta-blocker as an active principle for treating or improving obesity, metabolic diseases, and osteopenia. The composition according to the present application can prevent, improve and treat obesity, metabolic diseases including diabetes mellitus secondarily caused by obesity, and osteopenia/osteoporosis.
US20090123522 Medicament Delivery Device and a Method of Medicament Delivery A medicament delivery device and method of delivering a medicament is provided wherein the device is insertable into the uterine myometrium for the delivery of medicaments to the pelvic area and organs thereof, for example, the bladder, peritoneum, the vulva, vagina, fallopian tubes, ovaries, and uterus, and then to the bloodstream.
CN101002782A Medicine composition containing ceftin cyclodextrin clathrate, and its preparing method An inclusion compound of cefuroxime axetil with high solubility, stability and activity contains cefuroxime axetil and the pharmacologically acceptable cyclodextrin chosen from alpha-cyclodextrin, beta-cyclodextrin, gamma-cyclodextrin and their derivatives. Its preparing process is also disclosed.
CN102210682B Application of tetrahydropyrimidine and derivatives thereof in preparing medicament for treating cystitis The invention discloses a new application of 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinyl carboxy and derivatives thereof in the medicine field, namely an application in preparing a medicament for treating cystitis caused by chemotherapeutics. Found by the inventors surprisingly under study, 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinyl carboxy and derivatives thereof have an amazing therapeutic action on treating the cystitis caused by chemotherapeutics, and are favorable for alleviating pain of patients taking chemotherapy and for improving the tolerance dose of the patients on the chemotherapeutics, so that the tetrahydropyrimidine and derivatives thereof can be used for preparing the medicament for treating cystitis caused by chemotherapeutics. The invention also provides a medicament for treating cystitis caused by chemotherapeutics, composed of the tetrahydropyrimidine or the derivatives thereof and medically acceptable pharmaceutical auxiliary materials. Compared with the existing medicaments such as mesna and the like, the tetrahydropyrimidine and derivatives thereof have extensive therapeutic actions on the cystitis caused by chemotherapeutics rather than have limited preventiveactions.
CA2640655A1 Anaplastic lymphoma kinase (alk) as oncoantigen for lymphoma vaccination Use of intracytoplasmatic domain of Anaplastic Lymphoma Kinase (ALK) protein and/or a nucleic acid molecule encoding for the intracytoplasmatic domain of Anaplastic Lymphoma Kinase (ALK) protein, of any species, for the preparation of a medicament, preferably a vaccine, for the treatment and/or prevention of a tumor in a subject, preferably a lymphoma.
US7196108 Bicyclic heterocycles for the treatment of diabetes and other diseases The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.
US20120263754 Methods for Enhancing Immunogen Specific Immune Responses by Vectored Vaccines Provided herein are methods for inducing a specific immune response in a subject by administering to the subject an immunogenic composition comprising a recombinant expression vector, or a vector particle comprising the recombinant expression vector, which vector comprises a polynucleotide sequence that encodes an immunogen of interest. The methods further comprise administering an adjuvant composition either concurrently or sequentially with the immunogenic composition.
US20060246587 Methods for transfecting T cells A method for transfecting T cells with a nucleic acid molecule comprising a gene such that the gene is expressed in the T cells is described. The T cells are stimulated and proliferating prior to introduction of the nucleic acid molecule.
US6953809 Monocyte chemoattractant protein-1 inhibitor compounds The invention concerns the use of a compound of formula (I), in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, in the treatment of a disease or condition mediated by monocyte chemoattractant protein-1 (MCP-1). Certain of the components of formula (I) are novel and are provided, together with pharmaceutical compositions thereof, as further features of the invention.
WO2014126454A1 A process for producing high oleic content liquid palm oil fraction A process for producing high oleic content liquid palm oil fraction wherein the process includes subjecting substantially moisture-free palm oil to heat resulting in molten palm oil, lowering the temperature adding catalyst into the molten palm oil to initiate directed interesterification reaction, subjecting the oil-catalyst mixture to react at directed interesterification temperature, deactivating the catalyst, removing the catalyst from the directed interesterified palm oil, purifying the catalyst-free directed interesterified palm oil, subjecting the purified directed interesterified palm oil, crystallizing the molten directed interesteritified palm oil form high oleic content liquid palm olein and high palmitic content solid stearin fractions and separating the high palmitic content stearin solid crystals resulting in high oleic content liquid palm oil fraction.
CN102846563A Injection composition of pemetrexed disodium and preparation method of injection composition The invention relates to an injection composition, and in particular relates to an injection composition of pemetrexed disodium and a preparation method of the injection composition. The injection composition is prepared from pemetrexed disodium, mannitol and beta-cyclodextrin. The injection composition of pemetrexed disodium is simple in preparation process and effectively reduces the preparation cost. The pemetrexed disodium freeze-dried powder prepared by the invention has the advantages of excellent dissolvability, few impurity content, low moisture content and good stability.
CN102397508A Application of Tibetan medicine composition to preparation of medicament for treating bronchial asthma The invention discloses application of a Tibetan medicine composition to preparation of a medicament for treating bronchial asthma. The Tibetan medicine composition consists of the following raw materials in parts by weight: 5 to 15 parts of lamiophlomis rotata, 2 to 10 parts of whin, 15 to 60 parts of turmeric, 7 to 20 parts of sichuan pepper, 5 to 15 parts of buffalo horn, 15 to 40 parts of myricariagermanica, 0.1 to 2.5 parts of safflower, 0.1 to 5 parts of borneol and 0.1 to 5 parts of camphor. In the invention, by further research on the pharmacology of the traditional Tibetan medicine composition, the Tibetan medicine composition disclosed by the invention is found to have good curative effect in treating bronchial asthma. Moreover, pure natural wild herbs produced in the Qinghai-Tibet Plateau are adopted in the Tibetan medicine composition. The Tibetan medicine composition is not added with any chemosynthetic stabilizer, has no toxic or side effects on a human body, is safe andeffective and is suitable for various people.
US7759353 Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment Disclosed are certain substituted spiro iminopyrimidinones and other compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R1, R2, R6a and R7, are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.
CN102885816A Application of compound 6-(4-chlorophenoxy)-tetrazolo [5,1-a] phthalazine to preparation of medicine for treating depression The invention relates to the use of a compound (shown in formula I) as a medicine for treating depression.
US20110318363 Specific TT virus sequences and chimeric TT virus host cell DNA molecules for use in diagnosis, prevention and treatment of cancer and autoimmunity Described are single-stranded new sequences of TT viruses, rearranged TTV sequences and hybrid molecules of a specific TT virus sequence and host cell DNA that are capable of replicating autonomously for use in diagnosis, prevention and treatment of diseases like cancer and autoimmunity. In addition, it relates to the use of such molecules as gene vectors and artificial chromosomes.
US20080153917 Sigma Receptor Ligands The present invention concerns phenylcyclopentylacetamides and phenylcyclopropylcarboxamides and analogues thereof, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
US20100279993 Pharmaceutical Propylene Glycol Solvate Compositions The invention relates to pharmaceutical compositions comprising propylene glycol solvates of APIs.
CN102772705A Quick-acting collateral-dredging swelling-dispersing pain-relieving tincture and preparation method thereof The invention discloses quick-acting collateral-dredging swelling-dispersing pain-relieving tincture and a preparation method thereof. The quick-acting collateral-dredging swelling-dispersing pain-relieving tincture is mainly prepared by the steps of mixing the raw materials in parts by weight, grinding and bottling, wherein the raw materials include pine needle, berba aristolochiae mollissimae, alangium platanifolium, fructus liquidambaris, garden balsam stem, chinaroot greenbrier, beehive, hematoxylon, red paeony root, carthamus tinctorius, castor bean, aconitum pendulum, unprocessed rhizoma pinelliae, unprocessed monkshood, unprocessed radix aconiti agrestis, unprocessed arisaema consanguineum schott, unprocessed nux vomica, thunder god vine, sargent gloryvine, radix clematidis, ligusticum wallichii, frankincense, myrrh, asarum heterotropoides, camphor and borneol. The quick-acting collateral-dredging swelling-dispersing pain-relieving tincture disclosed by the invention is simple in preparation method and is capable of effectively treating various neuralgia diseases and various pyogenic infections, such as prosopalgia, vascular headache, toothache, traumatic injury, rheumatic arthritis, cervical vertebra and lumbar spondylosis.
WO2007031349A1 Use of c3-c10 17alfa-esters of 9,11-dehydrocortexolone as anti-gonadotrophic agents. The present invention relates to the use of C3-C10 17α-esters of 9,11- dehydrocortexolone as agents for inhibiting gonadotrophin secretion. The present invention therefore relates to the use of C3-C10 17 α-esters of 9,11- dehydrocortexolone for the preparation of a medicine for the treatment of disorders associated with the secretion of gonadotrophin and with the corresponding pharmaceutical compounds. The present invention relates specifically to the use of 9,11-dehydrocortexolone 17α-butyrate.
CN1739518A Application of penehyclidine hydrochloride in preparing medicine he present invention relates to the application of penehyclidine hydrochloride in preparing medicine, and is especially the application of penehyclidine hydrochloride in preparing pre-narcosis medicine. Animal experiment and clinical observation prove the obvious gland secretion inhibiting effect of penehyclidine hydrochloride as pre-narcosis medicine. The present invention expands the medicinal use of penehyclidine hydrochloride.
CN103145665A 17-hydro-9-dehydro-14,17-cyclo-andrographolide-19-sulphate and its preparation method and use in drug preparation The invention discloses 17-hydro-9-dehydro-14,17-cyclo-andrographolide-19-sulphate or its salt, and its preparation method and use in drug preparation. The 17-hydro-9-dehydro-14,17-cyclo-andrographolide-19-sulphate or its salt has effects of bringing down a fever, diminishing inflammation and resisting viruses. The 17-hydro-9-dehydro-14,17-cyclo-andrographolide-19-sulphate or its salt does not change chemical properties of andrographolide and has characteristics of good water-solubility, high thermostability and low hemolysis, and guarantees the pharmacological activity of an andrographolide all-natural drug to the maximum degree. Medical and pharmaceutical researchers cannot know the above uses of the 17-hydro-9-dehydro-14,17-cyclo-andrographolide-19-sulphate in advance without related experiments.
CN103520089A Metronidazole expandable vaginal suppository, and preparation method and detection method thereof The invention relates to a metronidazole expandable vaginal suppository, and a preparation method and a detection method thereof. The expandable vaginal suppository comprises metronidazole, a matrix and an expansion carrier. The drug-containing matrix also includes a resin; a resin compound formed by the resin with metronidazole can improve stability of the suppository and cooperate with an acidifier to prolong effect time of metronidazole on the vagina, extend therapeutic effect and maintain the specific acid environment and self-cleaning function of the vagina; and the chitosan can promote the absorption of metronidazole by the vagina and improve the bioavailability of the suppository. The metronidazole expandable vaginal suppository employs seven unique technologies and has beneficial effects of prevention of outflow liquid and secondary infection.
CN1911210A Dispersing tablets of nizatidine, and its prepn. method A dispersing tablet of nizatidine is proportionally prepared from nizatidine, microcrystalline cellulose, low-substituent hydroxypropyl cellulose, alcohol solution of PVPK30, lactose, magnesium stearate, and aspartame. Its preparing process is also disclosed.
EP2405924A1 Plasma-adapted full electrolyte solution The present invention relates to an aqueous full electrolyte solution. In particular, the present invention relates to an aqueous full electrolyte solution that is especially suitable as a solution for intravenous infusion and for subcutaneous infusion because of the plasma adaptation of said aqueous full electrolyte solution. In addition to the full electrolyte solution itself, an electrolyte mixture, a method for producing the full electrolyte solution therefrom, and a drug that comprises the solution and optionally an active ingredient are also provided.
EP1824456A2 Micronised azodicarbonamide, the preparation and use thereof Azodicarbonamide (ADA) in the form of a dry micronised powder is characterised in that the particle size distribution of said powder consists of particles whose mean diameter (d50) is equal to or less than 2 µm and of particles whose diameter in 90 % (d90) is equal to or less than 4 µm. A method for the preparation and use of agent is also disclosed.
CN103341102A Preparation method of dermatitis treatment ointment A preparation method of a dermatitis treatment ointment comprises: taking phellodendron, ageratum, cattail pollen, stemona, radical lobelia, pleione formosana hayata, rhizoma atractylodis, rumex japonicus root, campsis grandiflora, dahurian angelica root and sophora flavescens, adding water accounting for 5-7 times by mass of the medicinal materials, decocting for 2-3 h, removing medicinal dregs, and concentrating the medicinal soup to obtain a stiff paste for a standby application; taking snake oil and stearic acid, heating and keeping the temperature at 80-90 DEG C, melting; taking boiling water equal to the stearic acia in mass, triethanol amine, glycerin and sodium benzoate, heating and keeping the temperature at 80-90 DEG C, then adding into the melted stearic acid and the snake oil, continuously stirring, when in a uniform state, leaving and cooling to an emulsus state, then adding borneol and alum when the temperature is reduced to 30 DEG C or less, grinding together to a fine pasty state, adding the standby stiff paste, stirring uniformly. The dermatitis treatment ointment prepared by the method is effective in treatment of dermatitis, eczema and the like, is convenient to use, and helps to avoid pathological changes and drug dependence possibly caused in use process of western medicines.
WO2013177484A1 Methods of treating depression and pain [0119] The present invention provides methods of treating and pharmaceutical compositions useful for treating a mood disorder or depressive symptoms associated with pain, inducing analgesia and treating pain in a subject by administering a pharmaceutically effective amount of an agent capable of one or more of increasing GluAl level, expression, concentration, or biological activity, increasing calcium permeable AMPA (a amino-3-hydroxy-5- methylisoxazole-4-propionic acid) receptor (CPAR) level, expression, concentration, or biological activity or potentiating a CPAR current. The agent may be an AMPA potentiator or ampakine. The agent may increase AMPA receptor currents by slowing the deactivation of open channels and may be, for instance, 2-pyrrolidinone, 4-[2-(phenylsulfonylamino)ethylthio]-2,6- difluorophenoxyacetamide (PEP A) or LY451646. The agent may also be a protein, RNA or DNA product.
CN101185637B Silybin dimer self-emulsifying microemulsion preparation and its manufacturing method A silibinin dimer self-emulsifying microemulsion preparation contains the self-emulsifying microemulsion of silibinin dimer and the components are silibinin dimer, fabaceous lecithin, isopropyl myristate (IPM) and tween 80; the mass ratio is that silibinin dimer: fabaceous lecithin: isopropyl myristate (IPM): tween 80=1:0.5-1.5:1-6:3-9. Grain size of the self-emulsifying microemulsion is smaller than 300 nm and average grain size is smaller than 100 nm, most grains of the self-emulsifying microemulsion are globular or rod-shaped. The invention exists in the forms of microemulsion or soft capsule. The prepared microemulsion of the invention has the advantages of small grain size, good dissolvability, good system stability, simple preparation method, suitable for mass production and significant effect on preventing hepatic injury. The invention discloses the preparation method thereof.
CN1682703A Sterilizing gel The present invention relates to sterilizing gel, and sterilizing gel containing chlorhexidine or its physiologically acceptable salt as active component. The sterilizing gel contains also stuffing, excipient, synergist and pH regulator.
CN101028272A Enticawer chewing tablets and their preparation A chewing tablet of entecavir for treating hepatitis B and its preparing process are disclosed. It has high biologic utilization rate and low by-effect.
US20080124277 Human and Mouse Targeting Peptides Identified by Phage Display The present invention concerns methods and compositions for in vivo and in vitro targeting. A large number of targeting peptides directed towards human organs, tissues or cell types are disclosed. The peptides are of use for targeted delivery of therapeutic agents, including but not limited to gene therapy vectors. A novel class of gene therapy vectors is disclosed. Certain of the disclosed peptides have therapeutic use for inhibiting angiogenesis, inhibiting tumor growth, inducing apoptosis, inhibiting pregnancy or inducing weight loss. Methods of identifying novel targeting peptides in humans, as well as identifying endogenous receptor-ligand pairs are disclosed. Methods of identifying novel infectious agents that are causal for human disease states are also disclosed. A novel mechanism for inducing apoptosis is further disclosed.
CN103130710A Anti-enterovirus 71 (EV 71) caprolactam aldehyde compound and preparation method and purpose thereof A structure general formula of a caprolactam aldehyde enterovirus 71 (EV 71) 3C protease inhibitor is as shown in chemical combination A, all variables in the structure are defined in an instruction book, and the compound effectively restrains or blocks the copy of the enterovirus 71. The invention relates to a compound with the structure as shown in formula (A), various types of optical isomers of the compound with the structure as shown in formula (A), drug active metabolites, officinal salt, solvate and discovery and application when the compound with the structure as shown in formula (A), the various kinds of optical isomers of the compound with the structure as shown in formula (A), the drug active metabolites and the officinal salt are used for preparing antiviral drugs for curing hand-foot-mouth virus infection diseases. The invention further relates to an intermediate and a synthetic method of preparing the compound with the structure as shown in formula (A).
CN102206217A Heterocyclic compounds for treating or preventing diabetes mellitus as dipeptidyl peptidase inhibitor The invention discloses a group of heterocyclic compounds for treating or preventing diabetes mellitus as a dipeptidyl peptidase (DPP-IV) inhibitor. The compounds can be used for preventing and treating symptoms, such as obesity, diabetes mellitus and the like, in particular type II Diabetes mellitus, caused by the dipeptidyl peptidase. Meanwhile, the invention also discloses the activity of the compound and a detecting method thereof; and active pharmaceutical ingredients are provided for the treatment of the type II diabetes mellitus.
CN102526010A Compound undecylenic nanoemulsion and preparation method thereof The invention discloses a compound undecylenic nanoemulsion, which is formed by the following raw materials in mass percent: 18.05%-38.62% of surfactant, 0-9.15% of cosurfactant, 0-3.50% of oil, 0.50%-5.18% of undecylenic acid, 0.50%-3.00% of cinnamyl aldehyde, 0.50%-3.00% of eugenol and the balance of distilled water, wherein the sum of the mass percents of the raw materials is 100%. According to the compound undecylenic nanoemulsion disclosed by the invention, the solubility of the undecylenic acid is enhanced, the drug stability and the bioavailability of the undecylenic acid are improved, and the metabolic time of the undecylenic acid in vivo is retarded; and the undecylenic acid is in compatible with the cinnamyl aldehyde and the eugenol, the antimicrobial spectrum is enlarged, the drug consumption is reduced, and the cost for drug consumption is lowered, so that the compound undecylenic nanoemulsion has broad market prospects in the medicine field.
US20120172380 Novel 4-(tetrazol-5-yl)-quinazoline derivatives as anti cancer agent The invention relates to substituted 4-(tetrazol-5-yl)-quinazoline derivatives of the formula-I, or pharmaceutically acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted 4-(tetrazol-5-yl)-quinazoline derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti-proliferative effect in a warm-blooded animal such as man.
CN101597288A 2-aminoacyl-Beta-3-formyol tryptophan benzyl ester and preparation method and application thereof The invention discloses 2-aminoacyl-Beta-3-formyol tryptophan benzyl ester and a preparation method and the application thereof. The structural formula of the 2-aminoacyl-Beta-3-formyol tryptophan benzyl ester is shown in the general formula I, wherein AA is selected from phenylalanine, alanine, glycin, arginine, aspartic acid, isoleucine, methionine, serine, tyrosine, threonine, leucine, tryptophan, valine, proline, glutamine, N carbobenzoxy-Lysine or p-methylbenzyl cysteine. The antitumor activity of the compound having the general formula I is evaluated by an S180 mouse model, and the experimental result shows that the compound having the general formula I has excellent antitumor function and the can be used as antitumor agent.
US20080268020 Ophthalmic Emulsions Containing Prostaglandins Cationic ophthalmic oil-in-water type emulsions, include colloid particles having an oily core surrounded by an interfacial film. The emulsion includes at least one cationic agent and at least one non ionic surfactant, the oily core including a prostaglandin selected from the group consisting essentially of latanoprost, unoprostone isopropyl, travoprost, bimatoprost, tafluprost, 8-isoprostaglandinE2, or a mixture thereof, for treating ocular hypertension and/or glaucoma. These emulsions have the property to increase the chemical stability of prostaglandins.
EP0974348B1 Visceral fat lowering agent A visceral fat lowering agent, a visceral fat accumulation inhibitor, and a body fat distribution improver, each comprising as the active ingredient a thiazolidine derivative represented by formula (IV) wherein A3 represents an optionally substituted phenyl or oxazolyl group.
US20120107317 Use of cytoplasmic c-myc for regulating immune responses The subject invention provides novel uses of cytoplasmic c-Myc for modulation of innate immune responses. The invention is based, at least in part, on the surprising discovery that cytoplasmic c-Myc, instead of nuclear c-Myc, modulates pro-inflammatory immune responses via its role as a positive feedback regulator. Specifically, the subject invention provides methods for treatment or amelioration of inflammatory diseases and/or immune disorders via inhibition c-Myc expression or its activity. Also provided are methods for the development of therapeutic agents for treating infection, inflammation, immune diseases and autoimmune diseases.
CN103191081A Vitamin E soft capsules and preparation method thereof The invention relates to vitamin E soft capsules and a preparation method thereof. The vitamin E soft capsules consist of an inclusion and capsule shells, wherein the inclusion comprises the following raw materials in parts by weight: 10 to 60 parts of natural vitamin E and 10 to 80 parts of maize germ oil. Compared with the prior art, the vitamin E soft capsules have the advantages of high safety, high absorption, strong pertinence and the like.
CN103446175A Applications of water-soluble amino sugar in preparation of medicaments and health-care products for treating hyperuricemia, gout and nephropathy The invention discloses applications of water-soluble amino sugar in preparation of medicaments and health-care products for treating hyperuricemia, gout and nephropathy. The water-soluble amino sugar is water-soluble amino polysaccharide or water-soluble amino oligosaccharide. Experiments prove that the water-soluble amino sugar has effects of remarkably reducing the content of organism Serum creatinine SCr, blood urea nitrogen BUN and uric acid UA, relieves the injure of high-purine diet to the renal function, and has the effect of protecting the renal function. According to the technical scheme, the water-soluble amino sugar can be used for preparing medicaments and health-care products for treating and preventing hyperuricemia, gout and nephropathy and has bright market prospects.
CN101259107A Abuterluo tablet for treating chronic liver fibrosis and preparation technique thereof The invention relates to an Abuteluo tablet used or curing hepatic fibrosis caused by chronic hepatitis and a preparation method thereof, pertaining to the field of medicine and preparation technique of medicine. The Abuteluo tablet comprises medicines by weight portion: 1 portion of resveratrol taken as raw material drug and 0.2 portion of co-disintegrant, 0.08-0.2 portion of disintegrant, 0.1-0.12 portion of surfactant and 0.5-0.6 portion of adhesive which are taken as auxiliary materials. The Abuteluo tablet can swell and disperse quickly in water to lead the resveratrol to dissolve quickly, so that the dissolubility and the bioavailability of the Abuteluo tablet are greatly improved, ensuring the effective curative function. The technical problem that the invention aims at solving is to provide a tablet with good curative effect and high bioavailability to cure the hepatic fibrosis caused by chronic hepatitis and a preparation method thereof.
US20100303785 Novel therapeutics based on tau/microtubule dynamics The invention is based on the discovery of a novel neuroprotective peptide. In addition, the invention rests on the discovery that the NAP peptide enhances the association of tau and the brain-specific beta tubulin subunit. In addition, NAP modifies microtubule assembly and dynamics, in part, by affecting the tyrosination of microtubule proteins. The invention provides compositions and methods for treatment and prevention of neuronal disorders, including NAP-binding and tau-binding agents, tau peptide mimetics, NAP-like and NAP-like tau peptide mimetics.
CN102885785A Adriamycin-containing nanometer medicament microspheres and preparation method thereof The invention discloses adriamycin-containing nanometer medicament microspheres, which comprises adriamycin, nanoparticles, a polymer and medicinal auxiliary materials. The invention further provides a preparation method of the microspheres. The method comprises the following steps of: preparing adriamycin and the medicinal auxiliary materials into a nanometer medicament; adding the nanometer medicament into a polymer-containing organic solvent mixed solution for emulsifying; adding a nanometer medicament-in-oil mixed suspension into a water mixed suspension containing nanoparticles or containing nanoparticles and a surfactant for emulsifying to obtain an oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil compound emulsion; and curing the obtained compound emulsion, and centrifugally collecting microspheres. An appropriate polymer material and an appropriate microsphere preparation method are selected, the prepared microspheres have high envelop rate, and a layer of self-assembled nanoparticles on the surfaces of the microspheres has the effects of improving cell adhesion and reducing inflammation and microencapsulation caused by local excessive acid and hydrophobic materials. The method disclosed by the invention can be applied to preparation of other medicament slow release or controlled release microspheres.
US20120208806 Hsp90 Inhibitors The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.
US7091205 Use of tetramethylpyrazine in the treatment of brain tumor The present invention relates to the use of tetramethylpyrazine (TMP) in the treatment of brain tumor.
US20130022570 Crosslinked polyvinylamine, polyallylamine, and polyethyleneimine for use as bile acid sequestrants The present invention provides a crosslinked amine and amide polymers effective for binding and removing bile salts from the gastrointestinal tract. These bile acid binding polymers or pharmaceutical compositions thereof can be administered to subjects to treat various conditions, including hypercholesteremia, diabetes, pruritis, irritable bowel syndrome-diarrhea (IBS-D), bile acid malabsorption, and the like.
US6849637 Matrix metalloproteases (MMPs) inhibitors such as benzyl 4-benzyl-5-oxo-4H-(1,2,4)triazolo(4,3-a)quinazol-7-ylcarboxylate for inflammatory conditions such as rheumatoid arthritis or osteoarthritis, or cancer A compound selected from those of formula (I): in which: W represents N or C—R1; in which R1 is as defined in the description, X represents N or C—R2 in which R2 is as defined in the description, Y represents a group selected from oxygen, sulfur, —NH, and —Nalkyl, Z represents a group selected from oxygen, sulphur, —NR8 in which R8 is as defined in the description, and optionally carbon depending the definition of Y, n is an integer from 0 to 8 inclusive, Z1 represents a group —CR9R10 wherein R9 and R10, are as defined in the description, which group contains optionally multiple bonds or heteroatomes, A represents a cyclic group, m is an integer from 0 to 7 inclusive, the group(s) R4 is (are) as defined in the description, R3 represents a group selected from hydrogen, alkyl, alkenyl, alkynyl, and the group of formula: in which p, Z2, B, q, and R13 are as defined in the description, optionally, its racemic forms, isomers thereof, N-oxydes thereof, and its the pharmaceutically acceptable salts thereof, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.
CA2812043A1 Pyrimidinedione anti-viral compounds Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG- I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
WO2006122401A1 Negative regulation of nk cell functions by eat-2, a sap-related adaptor expressed in innate immune cells The present invention relates to the identification EAT-2 and ERT as novel therapeutic targets for the modulation of innate immune cell functions. More particularly the present invention describes novel methods for modulating innate immune cells-mediated immune response, useful in the treatment of cancer, infectious diseases as well as autoimmune diseases The invention also features EAT-2 deficient and overexpressing transgenic animals, screening assays to identify agents that modulate EAT-2 and ERT activity or expression as well as methods of treatments comprising a modulation of NK cells function
US7241785 Five-membered heterocyclic alkanoic acid derivative The present invention relates to a compound represented by the formula wherein R1 is an optionally substituted 5-membered heterocyclic group; X is a bond etc.; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; Y is a bond etc.; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n—Z1— (n is an integer of 0 to 8 and Z1 is a bond etc.) and the like; ring B is a 5-membered heterocycle optionally further having 1 to 3 substituents; W is a divalent saturated hydrocarbon group having 1 to 20 carbon atoms; R2 is —OH etc., or a salt thereof. A pharmaceutical composition containing this compound is useful as a prophylactic or therapeutic agent of diseases such as diabetes mellitus and the like.
CN1938016A Use of benzonaphthoazulenes for the manufacture of pharmaceutical formulations for the treatment and prevention of central nervous system diseases and disorders The present invention relates to the use of compounds from the group of benzonaphthoazenes and of their pharmaceutically acceptable salts and solvates for the manufacture of a pharmaceutical formulation for the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other transmitters.
US20110182988 Gastroretentive pharmaceutical dosage form This invention relates to an orally administrable, gastroretentive pharmaceutical dosage form which contains at least one pharmaceutically active ingredient and at least one polymeric adjuvant. The adjuvant serves to retain the dosage form in a selected region of the gastrointestinal tract for sufficient time for the pharmaceutically active ingredient to be released and absorbed. Ideally the dosage form will contain two or more pharmaceutically active ingredients which are delivered to different regions of the gastrointestinal tract.
US20100172958 Wound dressing devices and methods The present invention provides an absorbent wound dressing assembly that can be used to stanch, seal, or stabilize a site of tissue injury, tissue trauma, or tissue access. The wound dressing assembly is flexible so that it can be adapted and used to fit in narrow and small wound sites. Generally the wound dressing assembly comprises a flexible carrier material that is impregnated with a non-mammalian material for control of severe bleeding. The preferred non-mammalian material is poly [β-(1→4)-2-amino-2-deoxy-D-glucopyranose] more commonly referred to as chitosan.
WO2010110684A1 Nitric oxide donors The invention relates to triphenylphosphonium thionitrite compounds that selectively deliver nitric oxide (NO) to the mitochondria. The compounds of the invention comprise a lipophilic triphenylphosphonium cation linked to a thionitrite moiety via a linker group and a pharmaceutically acceptable anion. The compounds are useful in the treatment of diseases affected by indication of NO activity such as cancers, heart conditions, cognitive disorders and stroke.
CA2479737C Nanoparticulate compositions of map kinase inhibitors Nanoparticulate compositions comprising at least one poorly soluble MAP kinase inhibitor and at least one surface stabilizer are described. The nanoparticulate compositions have an average particle size of less than about 2000 nm. The invention also describes methods of making and using such compositions.
EP2678011A1 Antitumoral combination comprising cabazitaxel and cisplatin The present invention relates to a combination comprising cabazitaxel and cisplatin. The present invention relates also to a pharmaceutical composition containing such a combination and to a pharmaceutical kit comprising: (i) a first galenic formulation comprising cabazitaxel; and (ii) a second galenic formulation comprising cisplatin. The invention relates also to the use of this combination and/or pharmaceutical composition and/or pharmaceutical kit in the treatment of neoplastic diseases, more particularly in the treatment of cancer.
EP2641596A1 Use of 1,3-diphenylprop-2-en-1-one derivatives for treating liver disorders The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as aminotransferases . The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.
WO2008157802A1 3-hydroxyisothiazole-4-carboxamidine derivatives as chk2 inhibitors This invention provides compounds of Formula (I), which are inhibitors of Chk2 and are useful as a radiation protection agents in anticancer radiotherapy. A method of modulating Chk2 in vitro includes treating a substrate with Chk2 in the presence of compounds of formula I. A method of making a compound of formula I includes: a) forming a biaryl amine having an amino (NH2) group; b) converting the amino group to an isothiocyanate group; c) adding a cyanoacetamide to said isothiocyanate group to form a thioamide adduct; d) cyclizing said thioamide adduct to form an isothiazole having a cyano group; and e) adding an amine to said cyano group to form a carboxamidine group.
WO2010027028A1 Agent for ameliorating impaired brain function Disclosed are an effective and highly safe agent or pharmaceutical preparation for ameliorating various disorders caused by an impaired brain function, and others. Specifically disclosed are: an agent for preventing or ameliorating an impaired brain function, which comprises N-acetyl-D-mannosamine; a pharmaceutical composition for preventing, ameliorating or treating a disorder caused by an impaired brain function, which comprises an effective amount of N-acetyl-D-mannosamine and a pharmaceutically acceptable carrier; and a food containing N-acetyl-D-mannosamine.
CA2730734A1 Deuterated benzylbenzene derivatives and methods of use Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by SGLT inhibition.
US20140163062 Remedy for psychoneurotic diseases A medicinal preparation for preventing and/or treating psychoneurotic diseases such as integration dysfunction and Alzheimer's disease which contains tropisetron or its pharmaceutically acceptable salt as the active ingredient.
US20110190566 Polymer microgel beads The present invention relates to polymer microgel beads having a polymeric matrix with nanomagnetic particles dispersed substantially uniformly therethrough, wherein a steric stabiliser is associated with the particles, the steric stabiliser being a polymeric material that (i) does not form part of the polymeric matrix of the beads, and (ii) comprises a steric stabilising polymeric segment and an anchoring polymeric segment, wherein the steric stabilising polymeric segment is different from the anchoring polymeric segment, and wherein the anchoring polymeric segment has an affinity toward the surface of the nanomagnetic particles and secures the stabiliser to the particles.
CN101062085A Condyloma acuminata treating medicine The invention relates to a medicament for treating verruca acuminate which is prepared from raw material herbs of globe thistle 15-38, borneol 1-5, brucea fruit 5-25 and licorice root 5-25. The medicament can be prepared into externally used liniment.
US20080166301 Therapy for hormone sensitive diseases; side effect reduction; anticancer agents; osteoporosis; endometriosis; benign prostatic hyperplasia; cardiovascular disorders; acne The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorder. In an aspect of the invention, such treatments include therapeutic compositions comprising novel steroidal antiestrogen and antiandrogen compounds. In a preferred aspect, such a novel compound of the present invention has an address and a message component, which are made into a single composite entity for more aggressive intervention and effective treatment of hormone-responsive disorders, thereby prolonging the disease-free interval for the patient and reducing a number of side effects.
EP1140106B1 Treatment of diseases involving cyst formation The invention concerns the use of ligands of peripheral-type benzodiazepine receptors (PTBR) in the diagnosis and treatment of diseases involving cyst formation and in particular polycystic kidney disease. The invention further concerns the treatment of hypertension accompanying polycystic kidney disease, and pharmaceutical compositions and articles of manufacture for the treatment or diagnosis of the target disease or condition.
CN103330751A Natural medicinal composition and preparation method and application thereof The invention relates to a natural medicinal composition and a preparation method and application thereof. The natural medicinal composition consists of astragalus root-plantain seed decoction concentrate extract, astragalus root polysaccharide and plantain seed polysaccharide in a ratio of (2-6): (3-7): (1-7). The composition has an extremely good treatment effect on cancer chemotherapy-associated diarrhea and has a synergistic effect on cancer chemotherapy at the same time.
CN1795927A Composite of total flavone phospholipid of safflower, and preparation method A safflower flavone-phosphatide composition for resisting against virus, inflammation and anaphylaxis and benefiting gallbladder and urination is prepared from the safflower flavone and phosphatide in mole ratio of 1: (0.5-2) through mixing, dissolving in the organic solvent with low dielectric constant while stirring, filtering, and vacuum (or freeze) drying.
WO2008042735A1 Tetrahydroquinoline, indoline, and related aniline derivatives of heterocycle-fused benzodioxan methylamines The present invention relates to a compound of the formula: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, useful as modulators of 5 -HTi A receptor activity and/or serotonin reuptake. These compounds are useful in treating nervous system disorders, such as anxiety-related disorders, cognition-related disorders, depression, schizophrenia, or sexual dysfunction and related illnesses.
US20120264764 Oxabicycloheptanes and Oxabicycloheptenes, Their Preparation and Use This invention provides compounds having the structure which may be used for the treatment of tumors.
US20050118244 penetration promoter; hormone replacement therapy; contraception The invention relates to transdermal therapeutic systems containing at least one steroid hormone and propylene glycol monocaprylate as permeation enhancers. The invention also relates to methods for the production of said systems and to the use of the same in hormone substitution therapy and contraception.
EP1399188B1 Perylenequinones for use as sonosensitizers The invention is perylenequinones that are both sonosensitizers and photosensitizers, and their therapeutic use.
WO2013142831A1 Methods of making and using thioxothiazolidine and rhodanine derivatives as hiv-1 and jsp-1 inhibitors The present invention provides methods of making and using 5-(2-(indol-3-yl)-2-oxoethylidene)-3- phenyl-2-thioxothiazolidin-4-one derivatives having HIV- 1 or JSP- 1 inhibitory activity.
US20110065718 Antifungal Product, Use and Formulation Thereof An antifungal product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antifungal product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as two or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.
CN102711916A Use of an adrenal hormone-modifying agent The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or --C(O)N(Ra)(Rb) wherein Ra and Rb are independently --(C1-C4) alkyl, or --(C1-C4) alkyl-(C5-C7) aryl, wherein each of Ra and Rb is optionally substituted by --(C1-C4) alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or --(C6-C10) aryl, wherein said --(C6-C10) aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.
WO2012108397A1 Novel lipid The purpose of the present invention is to provide a novel cationic lipid which forms lipid particles. Provided are: a compound represented by formula (I); lipid particles which contain the compound; nucleic acid lipid particles which contain the lipid particles; and a pharmaceutical product which contains the nucleic acid lipid particles as an active ingredient.
CN101684108B 2-(3-cyano-4-isobutoxy phenyl)-4-methyl-5-thiazole formic acid and composition thereof The invention relates to a crystal form of 2-(3-cyano-4-isobutoxy phenyl)-4-methyl-5-thiazole formic acid (febuxostat) and a preparation method thereof, and the invention also relates to a medicinal composition containing the crystal form and application of the new crystal form in manufacturing medicaments for treating diseases caused by over-high uric acid.
WO2008116845A1 Piperidinone carboxamide derivatives as p2x7 modulators The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: (formula I) The compounds or salts modulate P2X7 receptor function and are capable of interfering with the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
WO2007128344A1 Design and synthesis of biotinylated probes for n-acyl-ethanolamines The present invention relates to the synthesis and characterisation of biotinylated analogue of N- arachidonoylethanolamine (AEA) and its use as a tool to study AEA transport and trafficking through biochemical and morphological techniques . In particular biotinylated AEA (b-AEA, for which we propose the common name MM22) is suitable to design highly sensitive and simple methods for the non-radioactive detection and quantitation of AEA from complex samples, which would offer a useful alternative approach to the routinely used radiometric assays. The invention also relates to the use of b-AEA as a potential therapeutic and diagnostic agent.
CN102430096A Medicament for treating rheumatic or rheumatoid diseases The invention relates to a medicament for treating rheumatic or rheumatoid diseases, which is prepared from the following crude drugs in part by weight: 50 parts of notopterygium root, 50 parts of radix angelicae pubescentis, 50 parts of radices sileris, 50 parts of processed Radix Aconiti, 40 parts of zaocys dhumnade, 60 parts of cortex acanthopanacis, 60 parts of radix angelicae, 40 parts of red flower, 50 parts of radix curcumae, 50 parts of rhizoma sparganii, 50 parts of Ligusticum wallichii, 60 parts of radix achyranthis bidentatae, 40 parts of frankincense, 40 parts of myrrh, 40 parts of borneol, 50 parts of Angelica sinensis, 30 parts of lumbricus, 60 parts of Astragalus mongholicus, 60 parts of ligusticum sinense oliver and 40 parts of ephedra. The medicament for treating the rheumatic or rheumatoid diseases has the effects of promoting blood circulation and removing blood stasis, eliminating swelling and stopping pains, removing dampness and clearing away cold, smoothing mainand collateral channels as well as removing toxin and relieving itching, and is capable of effectively treating the rheumatic or rheumatoid diseases.
US6841680 2-(Halophenyl)-quinoline derivatives for neuropathic pain; side effect reduction Compounds having selective action at neuronal N-type calcium channels useful for the treatment of pain in accord with the following structural diagram, wherein R1, R2 and R3 are a variety of groups as defined in the specification.
US20100144754 Methods and Compositions for Treating or Preventing Narcotic Withdrawal Symptoms This invention provides methods and pharmaceutical compositions for preventing or treating physical dependence and/or withdrawal associated with narcotic use, in particular by modulating a 5-HT3 receptor. Using a computational genetic approach in mice, a gene conserved between mice and humans was identified as candidate as a modulator of physical dependence to morphine. Administration of compounds that modulate 5-HT3 receptors was found to control withdrawal from morphine in mice and humans.
CA2602832A1 Low-concentration capsaicin patch and methods for treating neuropathic pain Described here are patches and methods for treating neuropathic pain. In some variations, the neuropathic pain-relieving patch comprises capsaicin or a capsaicin analog, wherein the concentration of the capsaicin or capsaicin analog is less than 1% by weight, and a penetration enhancer, wherein the patch is capable of relieving neuropathic pain over a sustained period of time. The penetration enhancer may be any suitable penetration enhancer. The patches may also include oils, viscosity increasing agents, and the like. In some variations, the pain-relieving patches comprise capsaicin, or an, wherein the concentration of the capsaicin or analog is less than 1%, and a penetration enhancer, whereby delivery of capsaicin from the patch continues for at least an hour, and whereby a single use of the patch provides a therapeutic benefit for at least one month, two months, or three months. Methods for treating neuropathic pain are also described.
US20110117032 Santising compositions and methods Sanitising compositions are provided for use in combination with cleaning compositions, cleaning and sanitization protocols with such compositions and applications of such sanitising compositions. The compositions comprise (a) biocidal component comprising one or more non-polymeric biguanides and analogs thereof, and one or more quaternary ammonium compounds and a formulation comprising (b) one or more cationic detergents having at least one unsubstituted alkyl group of 8 or more carbon atoms, (c) one or more chelating agents, and (d) an amine component comprising a mixture of at least one alkanolamine and at least one bis(aminoalkyl)alkylamine. The composition may be further enhanced by the incorporation of a mixture of surfactants comprises as a first component one or more non-ionic surfactants and as a second component one or more amphoteric surfactants. The composition is particularly effective when used in combination with a cleaning composition comprising the same mixture of surfactants.
CN1965893A Liquid formulation for treating allergic rhinitis Disclosed is a liquid preparation for treating anaphylactic rhinitis, wherein the constituents include (by weight percent) purple perilla oil 1.5-4.2%, methyl glycol 5-10%, Tween80 0.25-1.5%, Cremophor RH 40 5-15%, borneol 1-2%, lauryl alcohol 1-2%, isopropyl inosine 0.05-0.2%, uridylic acid 0.10-0.5%, sodium metabisulfite 0.1%, Ethylparabenum 0.2% and balancing distilled water to 100%.
US8198333 Cytostatic drug composition A drug composition containing as a drug substance a polymeric guanidine derivative based on a diamine containing oxyalkylene chains between two amino groups, with the guanidine derivative representing a product of polycondensation between a guanidine acid addition salt and a diamine containing polyalkylene chains between two amino groups, as well as the pharmaceutically acceptable salts thereof.
US20070260299 Covalent Grafting of Hydrophobic Substances on Collagen A hydrophobic grafted collagen, a method for preparing same and use thereof, in particular in therapy, are provided. Hydrophobic substances or molecules are grafted by covalent bonds on reactive amino acid residues of collagen molecules. The chemical linkages serve to modify the physico-chemical and biological properties of collagen and/or its derivatives. In particular, the introduction of hydrophobic residues enable the hydrophilic character of collagen to be modulated and its chemotactic properties involved in cell adhesion and growth to be modified.
US8343926 Therapeutic strategies for prevention and treatment of alzheimer's disease The invention relates to therapeutic agents for use in the prevention or treatment of Alzheimer's disease. In particular the invention relates to use of inhibitors of cell cycle re-entry and progression to the G1/S transition or inhibitors of progression of the cell cycle through the G1/S transition point in the prevention or treatment of Alzheimer's disease.
EP1915166B1 Marrubiin and composition for reducing snoring, package and method The invention comprises a composition for the reduction of snoring, a packaging therefor and a method for the manufacture thereof. The composition can be applied in the pharynx in different variants, in particular as spray, as gel or as foam formulation. In a preferred embodiment, the composition comprises White Horehound (Marrubium vulgare) and/ or black horehound (Ballota nigra). Application of the composition at least temporarily reduces the snoring of a treated person. The invention further comprises the use of marrubiin for the manufacture of a medication for the treatment of snoring.
WO2009049813A3 Process for producing a monophasic pharmaceutical product for limiting/reducing the risk of deep vein thrombosis united with oral contraception Monophasic oral contraceptives comprising a combination of 2.0 mg of dienogest and 0.030 mg of ethinylestradiol or 2.0 mg of dienogest and 0.020 mg of ethinylestradiol for nx21 daily dose units with subsequent, after nx21, use of a maximum of 7 daily intake-free or placebo-containing dose units, where n is equal to 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, and 17, achieve a limitation/reduction of the risk of deep vein thrombosis united with oral contraception. A suitable contraceptive composition with prolonged intake time of the hormone-containing daily dose units is provided and, despite the prolonged intake time, keeps the risk of deep vein thrombosis at the same level as with corresponding conventional oral contraceptives and thus within acceptable limits.
US8481548 2-[4-(2-chloro-pyridin-4-ylethynyl)-2-methyl-imidazol-1-yl]-4-trifluoromethyl-pyrimidine; metabotropic glutamate (mGluR5) receptor antagonist; analgesic, neurodegenerative diseases; psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognititve disorders, memory deficits, chronic and acute pain The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognititve disorders and memory deficits, as well as chronic and acute pain.
US8128972 Compositions and methods for enhancing and treating female sexual response The present invention relates to compositions, articles of manufacture, methods of preparation thereof, methods of use thereof, etc., for enhancement of sexual pleasure, conditions, disorders, and diseases related to reproductive physiology and systems, especially of mammalian females. For instance, the present invention relates to all aspects of modulating the female sexual response, including female sexual dysfunction, such as female sexual arousal disorders (FSAD), orgasmic disorders, and sexual pain disorders, and enhancing female sexual pleasure and satisfaction of the female sexual experience. Accordingly, the present invention relates to compositions comprising botanical extracts, active agents, etc., which are useful to treat or affect any of the aforementioned conditions. For example, the present invention relates to a composition, preferably for topical or local use, which comprises one or more of the following ingredients, including, but not limited to, borage seed oil, Angelica pubescens root and other angelica species, Coleus forskohlii extract, vinpocetine, ferulic acid, magnesium, ascorbyl palmitate, capric/caprylic triglyceride, silica, and equivalents thereof.
CN1817865A Preparation of sinomontanine and its hydrobromide Preparation of sinomontanine A and its hydrobromic acid salt are disclosed. The procedure is carried out by crushing block root of Gaowutou, extracting by alcohol reflux or acid water leakage or alcohol immersion, concentrating to thin paste to obtain crude extract, acidifying crude extract to pH=1í½5, obtain acidified liquid, adsorbing the acidified liquid by exchange resin cation or macroporous adsorbing resin or alumina, washing by water, washing by chloroform or/and alcohol, collecting eluent, concentrating extractive, dissolving the extractive into alcohol, laying aside for 1 day, crystallizing and washing by alcohol to obtain final product. It has higher purity.
WO2007047372A3 Pharmacological treatments for sleep disorders (apnoe) with prostanoid receptor antagonists This invention is directed to methods for preventing or ameliorating sleep-related breathing disorders. The method comprises administration to a patient in need thereof an effective dose of one or a combination of prostanoid receptor antagonists (eg. ramatroban, ifetroban, diphloretin, phosphate, polyphloretin phosphate, seratrodast, SC19220). The prostanoid receptor antagonist or combination of prostanoid receptor antagonists can be administered in conjunction with one or more serotonin receptor agonists, one or more cannabinoids receptor agonists, one or more serotonin reuptake inhibitors, one or more noradrenalin reuptake inhibitors, a combination of reuptake inhibitors, an inhibitor of prostanoid synthesis, or any combination of the foregoing.
US6891054 Functional acylglycerides The present invention relates to the field of human and animal nutrition, and in particular to certain novel compositions of conjugated linoleic acids (CLA). In particular, the present invention relates certain isomers of conjugated linoleic acids at either the SN1 and SN3 or SN2 positions of the acylglyceride molecule and another fatty acyl residue at the other of the SN1 and SN3 or SN2 positions of the acylglyceride molecule. These novel acylglyceride compositions containing conjugated linoleic acyl residues, medium chain fatty acyl residues, long chain fatty acyl residues, and ω3, ω6, and ω9 fatty acyl residues are efficacious as pharmaceutical compositions, animal feed additives, and human dietary supplements.
US20130011470 Pharmaceutical formulations of naproxen for soft gel encapsulation and combinations thereof An NSAID formulation for encapsulation into a soft gel capsule with increased stability, concentration and bioavailability of the NSAID. The preferred NSAIDS are naproxen, ibprofen, indomethacin and diclofenac, which are provided in both an acidic and basic form in the fill formulation. The pH values of fill formulations may be adjusted without additional process steps. A process for increasing the achievable concentration of an NASAID pharmaceutical ingredient in a fill composition for dosage units is also provided. The highly concentrated NASAID formulation permits a reduction in the fill volume or dosage unit size or an increase in concentration of the NSAID in each dosage it.
EP1140085B1 Azabicycloalkanes as ccr5 modulators Compounds of the Formula (I) [Region α] - [Region β] - [Region η] - [Region δ] which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formlations and methods of treatment using these compounds.
WO2013056264A2 Systems and methods for predicting response to anti-androgen therapy for the treatment of androgenetic alopecia Methods, processes, systems, and apparatuses are disclosed for predicting anti-androgen therapy response in the treatment of androgenetic alopecia based on a fluorometric assay and proteomics.
DE102007052119A1 New coumermycin A1-derivative, useful as biologically active substance and as antibiotics or cytostatics, and for preventing diseases caused by bacteria or tumor Coumermycin A1-derivative (I), is new. Coumermycin A1-derivative of formula (I), is new. R1, R2 : CH 3, halo or H, preferably H, F, Cl, Br or I, where both R1, R2 are not simultaneously CH 3. An independent claim is included for preparing (I). [Image] - ACTIVITY : Antibacterial; Cytostatic. - MECHANISM OF ACTION : None given.
CN103751148A Targeting and slow-release antineoplastic medicine nanoparticle with amphiphilic polyurethane as carrier and preparation method thereof The invention discloses a trgeting and slow-release antineoplastic medicine nanoparticle with amphiphilic polyurethane as a carrier and a preparation method thereof. The nanoparticle is of a nucleus-shell structure provided with two shell layers; a hydrophilic section of amphiphilic polyurethane serves as the shell layer, and a hydrophobic section serves as the nucleus; the nucleus covers the medicines; a functional molecule exposes from the surface of the shell layer of the nanoparticle; organo-siloxane can be hydrolyzed to form another shell layer between the hydrophilic section and the hydrophobic section; the medicines include capecitabine, adriamycin and paclitaxel; the functional molecule is folic acid; and organo-siloxane is tetramethoxysilane. The targeting and slow-release antineoplastic medicine nanoparticle with amphiphilic polyurethane as the carrier has the characteristics that degradable polymer materials are used as the medicine release-control preparations, which enables the medicine to act on a specified wound position with the minimum dosage; and the medicine release rate can be optimized to improve the treatment effect as well as reduce the toxic and side effects.
CN103182001A Microencapsulated high-ester type catechin-tea flavonoid crystal and its making method The invention discloses a microencapsulated high-ester type catechin-tea flavonoid crystal and its making method. The method mainly includes the steps of: 1. conducting ultrafine grinding on a tea raw material to obtain a catechin-tea flavonoid primary micropowder tea raw material; 2. maing a catechin-tea flavonoid crystal raw material; 3. carrying out high-speed centrifugal separation to obtain a high-ester type catechin-tea flavonoid crystal; and 4. preparing the microencapsulated high-ester type catechin-tea flavonoid crystal. The making method of the microencapsulated high-ester type catechin-tea flavonoid crystal grinds the tea raw material fine, maintains its original physicochemical properties, has high bioavailability, and the grinding process has certain sterilization function; through the high-speed centrifugal separation, loss of effective components of the tea raw material can be prevented, active components of tea leaves can be preserved, the technological process is shortened, and the cost is reduced; and the made high purity ester type catechin-tea flavonoid crystal is in favor of avoiding oxidation of catechin-tea flavonoid, and facilitates long-term storage and achievement of better antibacterial and antiviral effects.
US20110064711 Compositions containing coenzyme q-10 and an antioxidant The invention describes compositions of a reduced form of coenzyme Q-10 (CoQ10) or CoQ10 or both and an antioxidant that is an anthocyanin extract, a melanin or a compound having at least one thiol (—SH) group.
US6893642 Anticancer nutraceutical from spirulina The present invention provides a pharmaceutical composition containing proteoglycan extracts of algae and a process for preparing proteoglycan extracts from the algae.
US8198330 Therapeutic or prophylactic agent for diabetes, obesity, dyslipidemia or metabolic syndrome comprising benzylamine derivative or pharmaceutically acceptable acid addition salt thereof A method of treatment or prophylaxis of diabetes, obesity, dyslipidemia or metabolic syndrome includes administering an effective amount of a benzylamine derivative represented by Formula (I): wherein, R1 represents an alkyl group having 1 to 6 carbon atoms; R2 represents an alkyl group having 1 to 6 carbon atoms; R3 and R5 each independently represent a halogen atom, an alkyl group having 1 to 6 carbon atoms, a haloalkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and R4 represents a hydrogen atom or an alkoxy group having 1 to 6 carbon atoms, or a pharmaceutically acceptable acid addition salt thereof.
US20090124664 (R)-Arylalkylamino Derivatives and Pharmaceutical Compositions Containing Them The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
US20050004138 Overcoming phobias The present invention, in one aspect, relates to a method of using piperazinyl-heterocyclic compounds of the formula I, as defined below, for treating, in a mammal, including a human, situational anxiety, for example, anxiety experienced prior to medical procedures (e.g., surgery), public speaking, anxiety associated with swimming or water, anxiety associated with travel (e.g., air travel), or anxiety associated with specific phobias (snakes, spider, rats, sight of blood), comprising administering a pharmaceutically effective amount of a compound of formula I to the mammal. In another aspect, the present invention is directed to a method of using piperazinyl-heterocyclic compounds of the formula I, as defined below, for treating, in a mammal, including a human, treatment-resistant anxiety, which method comprises administering a pharmaceutically effective amount of a compound of formula I to the mammal. The compounds of formula I are defined as follows: or a pharmaceutically acceptable acid addition salt thereof, wherein Ar, n, X, and Y are as defined.
US20080032961 Therapy employing LXRalpha modolators The invention also relates to the use of active modulators of LXRα activity or expression in stimulation of pre-adipocyte differentiation and hence also in the treatment of insulin resistance syndrome, or dyslipidemia, or type 2 diabetes.
US20100240608 particle stabilised oil-in-water emulsion The present invention relates to an oil-in-water emulsion comprising a gelled particle emulsifier derived from naturally occurring food-grade polymers, the emulsion preferably being in the form of a food product or a home care product or a personal care product or a pharmaceutical product. Emulsifiers are limited in their use as they can cause allergic reactions in some people. There is thus a constant need for alternative emulsifiers. The goal of the present invention is to provide a stable emulsion which can be used in a wide number of applications. Thus an oil-in-water emulsion comprising 0.001-50%, preferably 0.001-30%, more preferably 0.001-10% w/w oil and 0.001 to less than 0.5%, preferably 0.001-0.4%, more preferably 0.01-0.4% w/w a gelled particle emulsifier, wherein the gelled particle emulsifier comprises at least one gellable polysaccharide, wherein the gelled particle emulsifier has a largest dimension of 3-1000 nm, preferably 5-500 nm, more preferably 10-200 nm, and wherein the emulsion composition does not comprise further emulsifier.
US20120208859 Novel mek inhibitors useful in the treatment of diseases The invention pertains to compound of Formula (I) wherein X, Y, Z, R1, R2, R3, R4, A and A′ are as described hereinabove. Formula (I) and (II) compounds can be used in pharmaceutical compositions, useful for the treatment of diseases.
US20050112668 Determination sensitivity for development fat metabolism diosrders by comparison of gene expression levels A method of determining whether a subject is suffering from or at risk for developing a disorder in fat metabolism. The method includes providing a sample from the subject and determining a Gsα expression level in the sample. If the Gsα expression level in the sample is different from that in a sample from a normal subject, it indicates that the subject is suffering from or at risk for developing a disorder in fat metabolism. Also disclosed are a method of identifying a compound for treating a disorder in fat metabolism, and a method and a composition for treating such a disorder.
CN101089008A Dicyclic analog without ring A and ring B of omithogalum caudatum OSW-1 saponin and its synthesis process and use The present invention provides dicyclic analog without ring A and ring B of Omithogalum caudatum OSW-1 saponin and its synthesis process and use. The synthesis process includes the following steps: 1. constituting dicycle; 2. region selectively reducing six-membered ring ketocarbonyl radical; 3. introducing 7alpha-hydroxy group; 4. Aldol reaction to introduce side chain and obtain 8alpha-hydroxy group; 5. oxidizing the position 7 hydroxy group into ketone; 6. turning the configuration of the position 7 hydroxy group; 7. glycosidating the position 7 hydroxy group; and 8. eliminating protecting group to obtain the target compound. The compound exhibits powerful antitumor activity and may be used in preparing medicine.
US20080069860 Administering a rare earth compound with calcium and aluminum salt or hydrophilic exchange resin in foods The present invention is generally related to the treatment of hyperphosphatemia in domestic animals. It is specifically directed to compositions containing phosphate binders that are palatable to domestic animals and methods using such compositions. In a composition aspect, the present invention provides a composition that includes: a rare earth compound (e.g., lanthanum oxycarbonate or lanthanum carbonate hydroxide), calcium salts (e.g, calcium carbonate or calcium acetate), aluminum salts (e.g., aluminum hydroxide or a hydrophilic exchange resin; and an ingredient of domestic animal food, wherein the ingredient is selected from a group consisting of chicken, beef, lamb, chicken meal or lamb meal, corn, rice, bone meal, fish meal, fish, egg product, beef, beef meal, corn gluten meal, poultry by-product meal, wheat flour, beef tallow, maple syrup, honey, apple, flaxseed, flaxseed meal, rice bran and germ, oats, barley, and wheat bran.
EP1817021A1 Nsaid compositions exhibiting clinical superiority The invention is directed to a composition and its use in treating pain, pyrexia and inflammation comprising an NSAIS as the active ingredient, a metasilicate, a first disintegrant and second disintegrant resulting in increased absorption of poorly soluble NSAIS’s and increased absorption in suppressed vagal systems. The preferred composition comprises ibuprofen on a metasilicate matrix, sodium bicarbonate as the first disintegrant and tartaric acid as the second disintegrant. The composition may also contain additional pharmaceutically acceptable excipients.
US20090012142 Compositions and Methods for Increasing Lean Muscle Mass and/or Reducing Fat Gain Compositions and methods for increasing lean muscle mass and/or reducing fat gain in growing animals by feeding the animals a composition having a total lysine to metabolizable energy ratio of from about 2.5 to about 6 g/Mcal and comprising (a) arginine in a total arginine to total lysine ratio of from about 1.1 to about 1.6; (b) isoleucine in a total isoleucine to total lysine ratio of from about 0.8 to about 1.3; (c) leucine in a total leucine to total lysine ratio of from about 1.8 to about 3.0; (d) valine in a total valine to total lysine ratio of from about 0.8 to about 1.4; and (e) methionine and cystine in a total methionine plus cystine to total lysine ratio of from about 0.8 to about 1.7.
WO2006030847A1 Novel bicyclic pyrazole derivative A compound represented by the following formula (I), a prodrug thereof, or a pharmaceutically acceptable salt of either. They have high DPP-IV inhibitory activity or have been improved in safety, nontoxicity, etc. [In the formula, R1 represents hydrogen, optionally substituted alkyl, etc.; the solid line and dotted line between A1 and A2 indicate a double bond or single bond; A1 represents nitrogen, etc.; A2 represents, e.g., a group represented by the formula C(R4) (R4 represents hydrogen, etc.); R6 represents optionally substituted phenyl, etc.; and Y represents, e.g., a group represented by the following formula (A): (wherein m1 is 0, 1, 2, or 3; and R7 is absent, or one or two R7's are present which each independently represents halogeno, etc.).]
CN101948428A 1-methyl-5H-indene (1,2-b) pyridine trifluoromethanesulfonic salt-5-(4-dimethylamino group) benzylidene derivative and preparation method thereof The invention belongs to the field of anti-tumor medicine preparation and in particularly relates to a 1-methyl-5H-indene (1,2-b) pyridine trifluoromethanesulfonic salt-5-(4-dimethylamino group) benzylidene derivative used as a DNA topoisomerase inhibitor and a preparation method thereof. The preparation method comprises the following steps of: (1) salifying reaction: stirring and reacting 5H-indene (1,2-b) pyridine and trifluoromethanesulfonic methyl ester in the molar ratio of 1:2-3 under the nitrogen protection at room temperature to obtain 1-methyl-5H-indene (1,2-b) pyridine trifluoromethanesulfonic salt; and (2) coupling reaction: distilling the 1-methyl-5H-indene (1,2-b) pyridine trifluoromethanesulfonic salt obtained in the step (1) with 4-dimethylaminobenzaldehyde in the molar ratio of 1.0:1.4-1.6 in glacial acetic acid to obtain the 1-methyl-5H-indene (1,2-b) pyridine trifluoromethanesulfonic salt-5-(4-dimethylamino group) benzylidene derivative. The obtained compound has strong function for inhibiting leukemia cell and human laryngeal squamous carcinoma. Besides, the preparation method has simple process and good productivity as high as about 65%.
US20100120760 Benzofuran-carboxamide derivatives as antiviral agents A compound of the formula (I): as defined herein, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing a compound of the formula (I) for use in inhibiting hepatitis C virus polymerase and/or of treating or preventing an illness due to hepatitis C virus,
US20120258117 Methods and compositions for modulation of histone ubiquitination Provided are methods and compositions for inhibiting mono-ubiquitination of a histone in a cell. Also provided are methods and compositions for inducing senescence in a cell. Additionally provided are methods and compositions for treatment of cancer, including glioma. In particular, these methods and compositions may include an inhibitor of a ubiquitin ligase.
US7265143 C-4 substituted retinoids C-4 substituted retinoic acid analogs, synthesis methods of C-4 substituted retinoic acid analogs and methods of using C-4 substituted retinoic acid analogs to treat various cancers and dermatological diseases and conditions. The C-4 substituted retinoic acid analogs include C-4 all-trans retinoic acid (ATRA) and 13-cis retinoic acid (13-CRA) analogs. The C-4 substituted retinoic acid analogs inhibit all-trans retinoic acid (ATRA) 4-hydroxylase activity, thereby inhibiting the catabolism of ATRA. The C-4 substituted retinoic acid analogs also have ATRA-mimetic activity. The preferred substitutions at C-4 are an azole group, a sulfur, oxygen, or nitrogen containing group, a pyridyl group, an ethinyl group, a cyclopropyl-amine group, an ester group, or a cyano group, or forms, together with the C-4 carbon atom, an oxime, an oxirane or aziridine group.
WO2014041446A3 Compositions and methods for treatment of metabolic diseases Provided are tetrahydrobiopterin compounds or their pharmaceutically acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. Also provided are pharmaceutical compositions comprising an effective amount of the above compounds used for treating or preventing metabolic diseases, which may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used for the treatment of phenylketonuria, cardiovascular disease, autism, ADHD, hypertension, endothelial dysfunction and chronic kidney disease.
CN101401859A Fever-lowering medicament for clearing heat and detoxication The invention discloses a medicament for clearing away heat and toxic material and allaying fever, which comprises raw materials in weight portion: 55 portions of baicalin, 60 portions of radix isatidis, 60 portions of honeysuckle, 40 portions of nacre, 15 portions of cholic acid and 20 portions of gardenia. The raw materials are weighed according to the weight portion, and can be made into granules, capsules or oral liquid by the prior method. The medicament has the advantages of clearing away heat and toxic material, inhibiting bacteria and reducing heat, resisting inflammatory and relieving analgesia, having no toxic and side effects, increasing immunity efficacy.
US20110033393 Hydrazone Compounds and Their Use The present invention relates to hydrazone compounds of Formula I: and pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3, R4, L1, and L2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I as inhibitors of TRPM5 protein.
CN102429921A Nipple protecting film (cow nipple protecting agent) The invention provides a cow nipple protecting agent. The protecting agent is formed by film forming fiber and various moisturizing agent and disinfecting agent. The protecting agent can form a protecting film, has a disinfecting effect, is no nonirritant, has no side effects and the film has good ventilation. After the milk of a cow is squeezed and the product provided by the invention is used, a layer of protecting film can be formed on the nipple in 3-5 minutes, so that bacteria can be prevented from invading, meanwhile, the disinfection function can be reached, and the mastitis can be effectively prevented.
CN103505740A Cyclodextrin mifepristone clathrate compound, preparation method thereof, and pharmaceutical composition containing clathrate compound The invention discloses a cyclodextrin mifepristone clathrate compound. The clathrate compound takes beta-cyclodextrin as a skeleton to include mifepristone; the ratio of the beta-cyclodextrin to the mifepristone is (1-5):1. Meanwhile, the invention discloses a preparation method of the clathrate compound, and a pharmaceutical composition containing the clathrate compound. The pharmaceutical composition is a solid preparation and comprises the cyclodextrin mifepristone clathrate compound and at least two auxiliary materials. The cyclodextrin mifepristone clathrate compound focuses on solving the problem of water-solubility of the mifepristone; the solubility of the cyclodextrin mifepristone clathrate compound in water is about 30 times of that of pure mifepristone; an oral preparation is prepared from the cyclodextrin mifepristone clathrate compound instead of the traditional mifepristone crude drug. Therefore, the absorption rate of the drug is greatly improved; the curative effect of the drug is greatly improved; the effect of drug metabolism is reduced; the toxic and side effects are reduced; the adaptability of a sufferer on the drug is increased.
CN100594036C Animal medicine capable of rehabilitating intestinal tract injury The invention relates to a animal medicine for restoring intestinal tract damage, wherein each 1000ml contains 500-5000mg solution of alpha-mannosan peptide, the solution contains antibiotics for anti-inflammation and eradicating pathogeny, the antibiotics including gentamicin, deoxytetracycline and Ofloxacin, the solution is prepared through subjecting preferred alpha-hemolytic streptococcus 33#to space embarkation, using fine bacteria through space mutagenesis seed selection as the production bacterial, carrying out first level fermentation and second level fermentation to produce mannosanpeptide fermentation liquor, purifying and filtering the fermentation liquor, charging right amount of perfume compound and flavoring agent, dissolving, stirring homogeneously and filtering again, loading and sealing, heat pressing and sterilizing.
CN1887259A Slow released compound anticancer prepn containing clorfarabine The slow released compound anticancer injection containing clorfarabine consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is the composition of clorfarabine and clorfarabine synergist selected from antitumor antibiotic and antimetabolite. The slow releasing supplementary material is polylactic acid/glycolic acid copolymer, polyethylene glycol, EVAc, etc. The .suspending agent is carboxymethyl cellulose, etc. and has viscosity of 80-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent. The present invention can inhibit the growth of tumor and enhance the curative effect of chemotherapy, radiotherapy and other non-operative treatment.
EP1828179B1 Nicotinic alpha-7 receptor ligands against cns-related diseases The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
US7192975 Arylimidazole derivatives, preparation and therapeutic used thereof Compounds of the formula wherein the substituents are as defined in the specification which are useful for the treatment of pain.
US20080171729 For an antiinflammatory agent, antiacne agent, antiproliferative agent, antiphototoxic agent, anti-hair loss agent, analgesic, antiaging agent, antiperspirant, antipruritic, astringent, or microbiocide; calcineurin inhibitors A method for enhancing skin permeability by administration of a tetracyclic compound and improved methods for treatment of disorders by administration of a tetracyclic compound and a pharmaceutically active compound.
CN1943575A Abuse potential low compound buprenorphin hydrochloride naloxone hydrochloride sublingual tablet A buprenorphine hydrochloride/naloxone hydrochloride sublingual tablets with low misuse potential , said tablets contain medicinal contents of buprenorphine hydrochloride and naloxone hydrochloride, part by weight thereof is 2:1-6:1, 1) using alcohol to dissolve regulator corrigent and bond of PH of prescription amount for use; 2) grinding main medicine buprenorphine hydrochloride/naloxone hydrochloride, filler and lubricant and sifting out thereof; 3) mixing evenly the prescription amount of buprenorphine hydrochloride/naloxone hydrochloride, filler, bond and disintegrating agent, thereafter adding contents in step 1 to prepare into soft stuff, again making into pellet, drying, sorting out, adding lubricant again, mixing evenly and pressing into tablet.
WO2008016288A1 Benzimidazo[1,2-c][1,2,3]thiadiazol-7-sulfonamides as inhibitors of carbonic anhydrase and the intermediates for production thereof The invention is related to novel compounds - benzimidazo[1,2-c][1,2,3]thiadiazole sulfonamides, corresponding to the general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression such as glaucome. The compounds of formula (I) inhibits enzymes such as carbonic anhydrases and metallo proteinases. This invention is also related to new intermediate compounds which are used for the synthesis of sulfonamides of formula (I).
CN101987125A Medicine for treating verruca plana and preparation method thereof The invention discloses a medicine for treating verruca plana, which is characterized by being mainly prepared from the raw materials in parts by weight: 1 to 20 parts of rose, 1 to 20 parts of seville orange flowers, 1 to 20 parts of purslane, 1 to 20 parts of herba patriniae, 1 to 20 parts of lithospermum, 1 to 20 parts of folium isatidis or isatis root and 1 to 20 parts of edible alcohol with the content higher than 95 percent. The medicine can be taken orally to be absorbed through the spleen and the stomach, can also be externally applied to be absorbed through the skin, and can be absorbed in a compound way of the oral taking manner and the external application manner. The medicine of the invention has the advantages of reasonable recipe, simple matching and accurate curative effect, and can treat both principal and secondary aspects of diseases. The invention also provides a preparation method of the medicine.
US20110256066 Method for preparing engineered mg doped ferrite superparamagnetic nano particle exhibiting ac magnetic induction heating at high temperature and mg doped ferrite superparamagnetic nano particles engineered by the method The present invention relates to a method for preparing a ferrite superparamagnetic nano particle engineered by magnesium doping, and a technique for applying it to hyperthermia cancer cell treatment and the heat shock protein (HSP) self-defense mechanism.
US20100266581 Compositions and methods for modulating s-nitrosogluthione reductase Disclosed herein are methods and compositions for modulating the levels and/or activity of S-nitrosoglutathione reductase (GSNOR) in vivo or in vitro. Specifically disclosed are GSNOR deletion constructs, host cells and non-human mammals comprising GSNOR deletions, and methods of screening employing GSNOR deletion mutants. Also specifically disclosed are reagents and procedures for measuring, monitoring, or altering GSNOR levels or activity (as well as nitric oxide and S-nitrosothiol levels) in connection with various medical conditions.
US20080199511 Vaginal or transdermal administering; therapy or contraceptives; polymer ring containing drug Disclosed are sustained release compositions for vaginal or transdermal administration that contain a progesterone receptor modulator such as CDB-2914 (also referred to as VA-2914), and methods of using them for long term contraception or therapeutic purposes. Also disclosed are methods for making the compositions.
EP2532668A1 Optically active 2-hydroxy tetrahydrothienopyridine derivatives, preparation method and use in manufacture of medicament thereof Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.
CN102134244A Medical photosensitizer and preparation method thereof The invention discloses a medical photosensitizer and a preparation method thereof. The photosensitizer is tetra(trifluoroethoxy) phthalocyaninate. The preparation method comprises: synthesizing an intermediate 4-trifluoroethoxybenzenedicarbonitrile by reacting 4-nitro-2-benzenedicarbonitrile with trifluoroethanol in dry dimethyl sulfoxide (DMSO) in the presence of lithium hydroxide; and reacting the intermediate and anhydrous metal chloride in dry n-amyl alcohol in the presence of 1,8-diazabicyclo[5,4,0]-undec-7-ene (DBU) which is a strong organic alkali to obtain the tetra(trifluoroethoxy) phthalocyaninate. In the method, the conditions are mild, the reaction temperature is only about 70 DEG C, and the yield is up to 78 percent. In-vitro cell experiments prove that the tetra(trifluoroethoxy) phthalocyaninate has high ability of killing HL-60 and SW-1116 cells. The results of in-vivo photodynamic therapy (PDT) tests show that ZnPcF has PDT effect on U14 transplantable tumor in mice and that the U14 transplantable tumor inhibition rate of the ZnPcF reaches 79.1 percent.
EP1373253B1 Inhibitors of cyclin dependent kinases as anti-cancer agent The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferation disorders such as cancer, leukaemia, psoriasis and the like.
US20080241129 Adipocyte secreted protein ccdc80 is a potent stimulator of bone formation Disclosed herein are methods of using Ccdc80, Ccdc80 mimics, or Ccdc80 agonists or antagonists in the treatment of bone disorders.
US20120183522 Biaryl pde4 inhibitors for treating inflammatory, cardiovascular and cns disorders The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders. The compounds have general formula I: A particular embodiment is
WO2014161938A1 Anti-tumoral composition comprising a pi3kbeta-selective inhibitor and a pi3kalpha-selective inhibitor The present invention concerns a combination of a PI3Kβ selective inhibitor with a PI3Kα selective inhibitor for use in the treatment of cancer.
WO2012097550A1 Cyclohydrocarbyl formamide derivatives, preparation methods and uses thereof Cyclohydrocarbyl formamide derivatives of general formula (I), preparation methods and uses thereof are provided. The present cyclohydrocarbyl formamide derivatives of general formula (I) target on the auxiliary protein Vif (Virus infection factors), and protect the natural anti-virus capability of APOBEC3G by inhibiting the function of Vif. And, new choices for the anti-HIV, anti-HCV or anti-HBV treatments are therefore provided.
WO2008011499A1 Synthesis of (2s,5r)-5-ethynyl-1-{n-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile A process for making (2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile and salts thereof, and intermediates used in the process are disclosed.
US20080171704 Composition and method for treating diabetes The present invention comprises dosing regimens and formulations of islet cell neogenesis associated protein (INGAP) and INGAP Peptide. The formulation disclosed herein is shown have acceptable stability as a pharmaceutical composition. Further, the formulation is able to regenerate functional islets.
CN101249184B Medicine for treating osteoproliferation as well as its preparation method The invention provides a medicine for treating hyperosteogeny and a preparation method. The invention is characterized in that the medicine is made by mixing raw ingredients with seed fat, wherein, the medicine has the raw ingredients by weight parts as follows: homalomena rhizome is 1 to 3, everflowering rose is 1 to 5, coralbean bark is 1 to 5, gentian is 1 to 2, herba lycopodti is 1 to 5, borneol is 0.1 to 1, rhizoma drynariae is 1 to 5, rhizoma ligustici wallichii is 1 to 3, radix bupleuri is 1 to 4, ground beetles are 1 to 3, radix paeoniae rubra is 1 to 3, roots of Spinyleaf Pricklyash is 1 to 3, and tibetan hellebore is 1 to 2. The medicine is pure TCM preparations, has no toxic side effects and low cost, cures the hyperosteogeny, and has stable curative effect and extremely low relapse rate.
US20070122475 Taste masking composition A composition for delivery of a medicament that has a bitter taste and/or causes throat catch is provided. The composition contains Carbomer 934, Carbomer 971, Carbomer 974, PEG-5M or a mixture thereof in an amount sufficient to mask the bitter taste of the medicament and/or throat catch.
DE20321153U1 Transdermal therapeutic system containing the analgesic fentanyl, comprising penetration accelerator-free drug-containing adhesive matrix of acrylate copolymer with hydroxyethyl acrylate and vinyl acetate units In a transdermal therapeutic system (TTS) comprising a covering layer, an adhesive matrix (AM) containing fentanyl (A) as active agent and a removable protecting layer, AM is of acrylate copolymer (I) containing hydroxyethyl acrylate and vinyl acetate units and is free of penetration accelerators and crosslinkers. - ACTIVITY : Analgesic. - MECHANISM OF ACTION : None given.
CN1771914A Freeze dried polyene lecithin powder for injection and its prepn The present invention discloses one kind of freeze dried polyene phosphatidylcholine powder for injection and its preparation process. It features that the preparation contains polyene phosphatidylcholine and solubilizer sodium deoxycholate, sodium dehydrocholate or sodium cholate in the weight ratio of 0.5-1.5.
US7550469 Heterocyclic amide derivatives and their use as dopamine D3 receptor ligands The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D3 receptors.
CN1795855A Medication for treating senilism dementia and preparing technique A medicine for treating presenile dementia is just the HA-T1 which is the huperzine A derivative N-methyl-1,4-dihydropyridine-3-formate or the HA-T2 which is the huperzine A derivative N-methyl-1,2,5,6-tetrahydropyridine-3-formate. Its preparing process is also disclosed.
CN1593458A Instant nutrition intensifying agent The invention provides an instant nutrition intensifying agent mainly comprising vitamin C, vitamin A, vitamins B, vitamins D, vitamin E, vitamins K, ferrum, Zinc, calcium, magnesium, copper, manganese, selenium, iodine, potassium, citric acid, fumaric acid, sodium hydrogen carbonate, anti-oxidant agent, excipient, and solubilizing agent.
CN103483226A Modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).
WO2010042646A1 Aza- and diaza-phthalazine compounds as p38 map kinase modulators and methods of use thereof The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I) wherein A1, A2, A3, A4, L, R1, R2, R3, R5 and m are as defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, ankylosing spondylitis, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).
US7439363 Substituted indazoly(indoly)maleimide derivatives as kinase inhibitors The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): R2 is selected from the group consisting of —C1-8alkyl-Z, —C2-8alkenyl-Z and —C2-8alkynyl-Z; wherein the —C1-8alkyl-Z, —C2-8alkenyl-Z and —C2-8alkynyl-Z and Z is a 5 to 6 member aromatic monocyclic heteroaryl ring having from 2 to 4 heteroatoms. These compounds are useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
WO2013147649A3 Inhibitors of the pi3k/akt/ikk/nf-kb signalling pathway, pharmaceutically acceptable salts thereof and compositions containing said inhibitors for the prophylaxis and treatment of viral diseases The invention relates to inhibitors of the PI3K/AKT/IKK/NF-kB signalling pathway, to analogues thereof and to pharmaceutically acceptable salts thereof, and also to pharmaceutical compositions containing said inhibitors for the prophylaxis and treatment of viral diseases. The invention is linked to methods for the prophylaxis and treatment of viral diseases using inhibitors of the PI3K/AKT/IKK/NF-kB signalling pathway, to analogues thereof, and to pharmaceutically acceptable salts thereof, and also to pharmaceutical compositions containing said inhibitors for the treatment of viral diseases and for the production of drugs.
US20080279905 Low irritation; containing ethylene-vinyl alcohol fibers and a crystal structure thermp[lastic resin To provide a fabric and clothing having a low irritation to patients with atopic dermatitis with high productivity. The fabric is produced as a fabric for patients with atopic dermatitis, which is contactable with an affected area of patients with atopic dermatitis and comprises an ethylene-vinyl alcohol (EVOH)-series fiber comprising an ethylene-vinyl alcohol-series copolymer having an ethylene content of 25 to 70% by mole, in which the surface of the EVOH-series fiber is occupied by the ethylene-vinyl alcohol-series copolymer in a proportion of not less than 70%, wherein the hydroxyl group amount of the EVOH-series fiber surface is 20 to 70% by mole, the Young's modulus of the EVOH-series fiber is not more than 60 cN/dtex, and the single fiber fineness of the EVOH-series fiber is not more than 5 dtex. The EVOH-series fiber may be a sheath-core structure conjugated fiber comprising the EVOH-series copolymer as the sheath component, in particular a sheath-core structure conjugated fiber which comprises the EVOH-series copolymer having an ethylene content of 25 to 70% by mole as the sheath component and a crystalline thermoplastic resin having a melting point of not lower than 150° C. as the core component.
CN1935151A Weight-reducing medicine or health product The present invention relates to a new slimming and slenderizing medicine or health-care product. It is characterized by that its effective active component contains 2-10 weight portions of puerarin and 2-10 weight portions of icariine. It can effectively reduce body weight of human body and reduce body fat content.
CN101234108A Pharmaceutical composition containing (3S, 2í»R)-3-(2í»-hydroxy-2í»-cyclopentyl-2í»-phenylethoxy) quinuclidine hydrochloride and uses thereof The invention discloses medical composition containing active component of (3S, 2'R)-3-(2'-hydroxyl-2'-cyclopentyl-2'-phenylethoxy) quinine quinuclidine chloride and application of the medical composition in preparing drugs for treating chronic obstructive lung disease, incontinentia urinae, diversified shock diseases and preparing adjuvant drugs used before anaesthesia. The active component of the medical composition of the invention has high optical purity, strong stereoselectivity in vivo process, definite curative effects and high pertinency to the disease, thus effectively avoiding generation of toxic and side effects.
CN102391107A Method for preparing gallic acid quinolone drug salt and preparation method thereof The invention relates to a method for preparing a gallic acid quinolone drug salt and a preparation method thereof. By adopting the method provided by the invention, a series of gallic acid quinolone drug salts are prepared, such as gallic acid norfloxacin, gallic acid ciprofloxacin, gallic acid ofloxacin, gallic acid levofloxacin, gallic acid prulifloxacin, gallic acid pefloxacin, gallic acid mosifloxacin and the like. The gallic acid quinolone drug salt prepared by the invention has pharmacological action of quinolone and also has the pharmacological action of gallic acid, two different pharmacological action mechanisms can realize synergic antibacterial action, and the gallic acid quinolone drug salt can be prepared into tablets, dispersible tablets and capsules used for oral administration and injection used for injection and also can be prepared into suppository and lotion which are used for local application (rectum application and vagina application). The quinolone drug is a broad spectrum antibiotic, and the gallic acid has antibacterial, antiviral and antitumour functions. The preparation method of the quinolone drug salt can mutually enhance antibacterial action after being applied.
WO2014139456A1 Application of aluminum hydroxide in preparation of medicament for treatment of liver cancer An application of aluminum hydroxide, Al(OH)3, as an individual component in preparation of a medicament for treatment of liver cancer. Inhibition of liver cancer cell growth is allowed, and, use in conjunction with other liver cancer prevention methods or anti-liver cancer medicaments is allowed.
US6890913 Novel chitosan of given degree of deacetylation and weight average molecular weight, production of chitosan from a fungus, and use of chitosan for treating breast or cervical cancer A chitosan having a weight average molecular weight of 50,000-140,000 g/mole and a degree of deacetylation of 85-95%. Also disclosed are a method of preparing a chitosan from a fungus, and a method of using a chitosan for treating breast or cervical cancer.
CN101559067A Pharmaceutical composition containing azithromycin for vagina The invention discloses a pharmaceutical composition containing azithromycin and pharmaceutically acceptable salts thereof for vagina, which are used for treating vagina inflammation.
CN101259187A Medicaments assembly for treating eczema and preparation thereof The invention relates to a medicine combination for treating eczema. The medicine combination is made of fructus xanthil, mhurricane lamp, kelp, angelica, rhizoma ligustici wallichii, herba schizonepetae, radix-polygoni multiflori, cicada ecdysis, Cortex Dictamni, Flemingia philippinensis, caltrop, raw rehmanniae, houttuynine sodium bisulfite, duckweed, gypsum, burdock, Chinese knotweed and or a carrier that is acceptable by pharmacy. The invention also relates to the preparation method of the medicine combination. The medicine combination used for treating eczema has the effects of clearing heat, promoting dieresis, nourishing the blood to expel wind and eliminating coldness and is used for treating severe itching and erosion caused, etc. caused by the eczema.
CN101675046A therapeutic agents The present invention is directed to therapeutic agents of the formula (I) which are atypical antipsychotics and which arc useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. wherein; R<1> is C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro, wherein R<1> and the hydroxyl group on the ringare attached to the same carbon atom; or a pharmaceutically acceptable salt thereof.
CA2649146A1 4-anilinoquinoline-3-carboxamides as csf-1r kinase inhibitors The invention relates to chemical compounds of formula IA or IB: formula IA IB or pharmaceutically acceptable salts thereof which possess CSF 1R kinase inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti cancer effect in a warm blooded animal such as man.
EP1210116B1 Pharmaceutical combination for the treatment of viral infections containing a calcium channel blocker and a quinoline A pharmaceutical composition comprising therapeutically effective quantities of calcium channel blockers in combination with quinolines. In preferred embodiments, the invention further comprises quercetin. The components combine and interact in a manner to effectively treat viral injections.
US20080085932 Pharmaceutical Compositions Useful In Prevention and Treatment of Beta-Amyloid Protein-Induced Disease The invention provides methods for treating beta-Amyloid protein-induced disease, pharmaceutical compositions and compounds useful for the same, and the use of these compounds for the manufacture of a medicament for treating the same. More particularly, the invention relates to the use of natural product compounds isolated from turmeric, gingko biloba, and ginger, and synthetic chemical analogues thereof, for the treatment of a beta-Amyloid protein-induced disease.
EP2262500A1 Thienopyridone derivatives as amp-activated protein kinase (ampk) activators The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).
CN101732525A Medicinal composition for postpartum recovery The invention discloses a medicinal composition for postpartum recovery. The medicinal composition is characterized by being prepared from the following raw materials in percentage by weight: 10-20 radix pseudostellariae, 5-10 hawthorn, 10-20 Chinese date, 5-10 rhizoma cyperi and a proper amount of brown sugar. The medicinal composition has reasonable formula and can effectively reduce the postpartum hemorrhage, promote lochia elimination and accelerate the involution of uterus proved by clinical use. In addition, the invention can accelerate the mental restoration of the physical strength of parturient, prevent the puerperal constipation, and help the parturient recover the figure.
US20080305132 Cosmetic Patch for Skin Treatment There is provided a treatment product (1) comprising a patch (3), said patch (3) comprising a polysiloxane as a treatment agent, and wherein the patch (3) is arranged such that it can be removeably adhered to a user's skin. Also provided are other treatment products, the use of polysiloxane for manufacturing a medicament and the use of polysiloxane to treat a cutaneous condition.
WO2008098977A1 Novel triazole derivatives as ligands of g-protein coupled receptors The present invention provides novel triazole derivatives according to Formula (I) as ligands of G-protein coupled receptors (GPCR), which are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, which are mediated by GPCR. The present invention further provides GPCR antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular adipogenesis, adiposity, cachexia, diabetes, diabetes type I, diabetes type II, energy balance, energy homeostasis, food intake, hyperlipidemia, hyperphagia, obesity, short-, medium- and/or long-term regulation of energy balance, short-, medium- and/or long-term regulation (stimulation and/or inhibition) of food intake.
US20110086898 Pyrazolooxazole compound A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism. wherein R1 and R2 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, a C1-6 alkyl group substituted with a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, etc; R3, R4 and R5 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C1-6 alkoxy-C1-6 alkyl group, a C3-6 cycloalkoxy-C1-6 alkyl group or a halogen atom; R6 is a hydrogen atom or a C1-6 alkyl group; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkylthio group.
US20100316589 Coated Pharmaceutical Compositions The present invention relates to polycarbophil coated crosslinked amine polymers and/or pharmaceutical compositions comprising polycarbophil coated crosslinked amine polymers. The polycarbophil coated crosslinked amine polymers have several therapeutic applications, including, but not limited to, hyperphosphatemia, chronic kidney disease and End-Stage Renal Disease.
EP2536282A1 Methods for treating infection The present invention provides new methods and kits for treating and preventing bacterial infection.
WO2010011349A3 Pyrimidine-2,4-diamines as jak2 kinase inhibitors for treatment of inflammation A method of treatment or prevention of Castleman's disease, atherosclerosis, coronary artery disease, peripheral edema, peripheral vascular disease, glaucoma, and wet or dry age-related macular degeneration (AMD), asthma; chronic bronchitis; chronic obstructive pulmonary disease; adult respiratory distress syndrome; infant respiratory distress syndrome; cough; chronic obstructive pulmonary disease in animals; adult respiratory distress syndrome; ulcerative colitis; Crohn's disease; hypersecretion of gastric acid; bacterial, fungal, or viral induced sepsis or septic shock; endotoxic shock; laminitis or colic in horses; spinal cord trauma; head injury; neurogenic inflammation; pain; reperfusion injury of the brain; psoriatic arthritis; rheumatoid arthritis; alkylosing spondylitis; osteoarthritis; inflammation; or cytokine-mediated chronic tissue degeneration comprises the step of administering a therapeutically effective amount, or a prophylactically effective amount, of a compound having the structure (I).
WO2014135123A1 17α-ethynyl-androst-5-ene-3β,7β,17β-triol ophthalmic preparation Provided are an ophthalmic preparation comprising 0.01 wt.% to 1.5 wt.% 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and a preparation method thereof. The ophthalmic preparation is used for treating ophthalmic diseases.
CN102018944A Repellent for preventing insects and animals from harming human body and plaster prepared from same The invention relates to a repellent for preventing insects and animals from harming a human body and a plaster prepared from same, which effectively repel insects and animals including mosquitoes, fleas, ants, flies, cockroaches, grub worms, scolopendras, scorpions, wasps, mice, snakes, wildcats and pi-dogs, are safe and harmless for the human body, and are environment-friendly. Active ingredients of the repellent are mixed with carboxymethylcellulose and starch to be prepared into a sustained-release repellent; the sustained-release repellent can be coated on sponge to form the plaster; and the sustained-release repellent also can be diluted and packaged into a spray bottle for direct spray so as to prevent the insects and animals from harming the human body in 12 hours.
US20120157371 High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
WO2008028662A1 N-[1-(3-amino-4-phenyl-butyryl)-4-hydroxy-pyrrolidin-2-ylmethyl}-propionamide and related compounds as dpp-iv inhibitors for the treatment of type 2 diabetes mellitus The invention relates to compounds of formula (I) and formula (II) wherein Z1 R1-5, R, W, X, Y, m, n and A1 have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.
CN102949397A Cefotaxime sodium and tazobactam sodium preparation for injection and preparing method thereof The invention discloses a cefotaxime sodium and tazobactam sodium preparation for injection and a preparing method thereof. The preparing method comprises the step that cefotaxime sodium and tazobactam sodium are mixed uniformly to prepare the cefotaxime sodium and tazobactam sodium preparation for injection, wherein the mass ratio of the cefotaxime sodium to the tazobactam sodium is 1-4:1. A product prepared throughin the preparing method has good uniformity, the operation is simple, no special devices are needed in the production, and the method is suitable for industrial production. The cefotaxime sodium and tazobactam sodium preparation for injection has good content uniformity and stable quality.
US20090041863 Use of GSK3 inhibitors in combination with radiation therapies The presently disclosed subject matter relates generally to the fields of molecular biology and medicine. More particularly, it concerns methods involving the use of GSK3 inhibitors in combination with radiation therapies. In some embodiments, administration of a GSK3 inhibitor to a subject results in an amelioration of cognitive decline, toxicity to vascular endothelial cells, and/or neuron death associated with radiation therapy alone.
WO2011014600A1 Methods of treating neuropathic pain with benzimidazole derivative agonists of ppargamma Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain with benzimidazole derivatives with PPARgamma agonist activity, as well as methods for preparing medicaments used in such treatments of mammalian pain.
US20090023720 2-Amino 1H-Imidazo Ring Systems and Methods 1H-Imidazo ring systems (e.g., imidazopyridines, imidazoquinolines, imidazonaphthyridines, 6,7,8,9-tetrahydro imidazoquinolines and imidazonaphthyridines) with an amino substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
US20080027084 antiinflammatory agent, anticarcinogenic agent; for treating inflammatory diseases, allergic, autoimmune, metabolic, cancer, cardiovascular diseases The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4 -ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein. Compounds that are useful intermediates of the process are also provided herein.
US20080317844 Pharmaceutical Delivery Systems for Hydrophobic Drugs and Compositions Compositions Comprising Same A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.
CN102885771A High-concentration vitamin C injection solution and preparation method thereof The invention discloses a high-concentration vitamin C injection solution, comprising vitamin C, ethylene diamine tetraacetic acid disodium salt, sodium metabisulfite, L-cysteine, sodium bicarbonate and water for injection, and further comprising sodium diethyldithiocarbamate, wherein the concentration of the vitamin C in the high-concentration vitamin C injection solution is 10-30 g/L, and the concentration of the sodium diethyldithiocarbamate is 0.4-1 g/L. Additionally, the invention further discloses a preparation method of the high-concentration vitamin C injection solution. According to the invention, a main medicine vitamin C can be protected not to be oxidized during a storage process by means of adding a stabilizer sodium diethyldithiocarbamate in the vitamin C injection solution and matching with sodium metabisulfite and the L-cysteine, thus greatly prolonging the validity period of the vitamin C injection solution; and the quality guarantee period of the vitamin C injection solution is prolonged to 48 months from 12 months by means of adopting a specific addition sequence during the preparation process.
US20120114729 Silicone-peroxide compositions for long-term, controlled oxygen release A composite for delivering extended-release of oxygen is disclosed. The composite can include a biocompatible polymeric support having a plurality of solid peroxide particles suspended therein. The polymer support can exhibit an oxygen tension value of at least 40 mmHg for a period of 14 days. The weight ratio of biocompatible polymeric support to solid peroxide particles can range from 1:1 to 99:1. Also disclosed is a method of using the composite to deliver oxygen to cells in both in vivo and in vitro environments.
US20130065861 Compounds (cystein based lipopeptides) and compositions as tlr2 agonists used for treating infections, inflammations, respiratory diseases etc. The invention provides a novel class of compounds viz. generally lipopeptides like Pam3CSK4, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness a vaccine.
CN102091323A Compound preparation of collagen powder and preparation method thereof The invention discloses a formula of a Beiai brand collagen powder and a preparation method thereof. 1,000 bags of Beiai brand collagen powder are prepared from 5,910 grams of collagen powder, 72 grams of vitamin C and 18 grams of honey peach essence, wherein each bag of collagen powder is 6 grams in weight. The preparation method comprises the following steps of: after raw materials and auxiliary materials pass quality inspection, preparing the collagen powder, the vitamin C and the honey peach essence according to the formula; mixing; performing split charging; performing external packaging; inspecting; and placing products into a storage to store. The Beiai brand collagen powder is applicable in the fields of food, medicaments and health-care products and is used for improving skin and beautifying.
US20120065221 Extended Release Oral Pharmaceutical Compositions of 3-Hydroxy-N-Methylmorphinan and Method of Use The present invention is directed to oral, therapeutically effective extended release pharmaceutical compositions of 3-hydroxy-N-methylmorphinan, including delayed onset, extended release dosage forms and the use thereof.
US7618986 Method of treating latent tuberculosis 2-Nitroimidazolyl-alkylaminoquinolines, and compositions containing the same, useful in the treatment of tuberculosis are disclosed. Methods of treating tuberculosis using the 2-nitroimidazolyl-alkylaminoquinolines, and compositions containing the same, also are disclosed.
WO2005020911A3 Benzo[1, 3]dioxole compounds, pharmaceutical compositions thereof, and processes of making and using the same The present invention relates to benzo[1, 3]dioxole compounds and pharmaceutical compositions containing such compounds. These compounds and compositions may be made by various methods. These compounds and compositions may be used to treat disorders and diseases such as cancer.
US20130089579 Combination of Hyaluronic Acid and Prilocaine A composition of matter comprising hyaluronic acid and/or a pharmaceutically acceptable hyaluronate salt, cross-linked hyaluronic acid and/or a pharmaceutically acceptable cross-linked hyaluronate salt, and prilocalne and/or a pharmaceutically acceptable salt thereof, and optionally at least one additive.
WO2006063805A1 3-amino-pyrazolo[3,4b]pyridines used as inhibitors of protein tyrosine kinases for treating angiogenic, hyperproliferative or neurodegenerative diseases The invention relates to compounds of general formula (I), in which R1 and R2 are described in the application, to the use of the compounds of general formula (I) as inhibitors of protein tyrosine kinases for treating various diseases, and to the compounds of general formulas (II) and (III) as intermediate compounds for producing compounds of general formula (I), in which X, R1a and R2a have the meanings as described in general formulas (II) and (III).
US20110275577 Methods of treating dermatologic, gynecologic, and genital disorders with caffeic acid analogs The present invention relates to caffeic acid analog compounds and methods which may be useful for regeneration, cellular programming, and the treatment of dermatologic, gynecologic, and genital diseases such as inflammatory dermatologic conditions, dysplasia, neoplasia, in situ carcinoma, invasive carcinoma, lichen sclerosus, lichen planus, vaginal dysplasia, vaginal carcinoma, vulvar dysplasia, vulvar carcinoma, cervical dysplasia, cervical carcinoma, and Kaposi's sarcoma.
CN103655764A Concentrated drug for treating gingivitis The invention discloses a concentrated drug for treating gingivitis. The concentrated drug consists of the following material medicine components in parts by weight: 20-30 parts of coptidis rhizome, 10-20 parts of rhizoma cimicifugae, 10-20 parts of scutellaria indica, 10-20 parts of indigo naturalis, 15-25 parts of gypsum, 1-5 parts of capsicum annuum, 1-5 parts of camphor, 1-5 parts of asarum, 1-5 parts of borneol, 0.1-0.5 part of musk, 20-30 parts of alum, 0.1-1 part of venenum bufonis and 0.1-1.5 parts of calculus bovis. The concentrated drug disclosed by the invention has obvious treatment effect on gingivitis, has extract curative effect, relives pain after being applied for 5-10 minutes, can cure the gingivitis in 15 days without relapse, and is worthy of popularization.
CN101066961A Flavone derivative and its prepn and use The present invention provides one kind of nitrogen atom-containing flavone derivatives, 2-substituent phenyl-5, 7-dioxy-8-amino methylene flavone derivatives, which are synthesized through introducing different amino methylene structures into the 8-position of flavone kernel. Pharmacological experiments shows that the 2-substituent phenyl-5, 7-dioxy-8-amino methylene flavone derivatives have extracorporeal inhibition on the proliferation of tumor cell strains, including Bel-7402, PC-3, ECA-109, A-549, HL-60, MCF-7, etc and cell period inhibiting effect and may be applied in antitumor medicine. The present invention has the general structural expression of the 2-substituent phenyl-5, 7-dioxy-8-amino methylene flavone derivatives shown.
US20100076075 Methods of treating neurological disease using antagonists of the nmda receptor complex Provided is a method for treating depression with an open-channel antagonists of the NMDA (N-methyl-D-aspartate) receptor complex. The open-channel antagonists include memantine (a 1-amino-3,5-dimethyl-adamantane hydrochloride), felbamate, acamprosate, and MRZ 2/579 (1-amino-1,3,3,5,5-pentamethyl-cyclohexane hydrochloride). The method includes oral, controlled or sustained release, intravenous, rectal, transcutaneous or other preparations such as lipid emulsion or crystal technology administration of the open-channel antagonist.
US7569212 Impregnation of contact lenses in a solution which comprises one or more suitable components for the treatment, care and/or protection of the eye A procedure for the manufacture of contact lenses for eye treatment, eye protection and eye-care wherein the lenses are impregnated with a suitable composition, a composition for the impregnation of a contact lens for the treatment and/or care and/or protection of the eye, and a kit containing such a composition and one or more contact lenses are disclosed herein. A method for the treatment and/or car and/or protection of the eye comprising wearing contact lenses impregnated with a suitable composition and a composition for disinfection and/or conservation of eye care products is also disclosed herein.
US20120258982 Adamantyl compounds The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
WO2008018825A1 Oral polyvinyl alcohol capsules comprising proton pump inhibitors The present invention relates to an oral pharmaceutical dosage form comprising a proton pump inhibitor characterized in that the dosage form is in the form of a capsule comprising a pharmaceutical formulation containing a proton pump inhibitor, optionally other pharmaceutically acceptable excipient(s) and optionally additional pharmaceutically active substance(s), and the capsule material comprises a polyvinyl alcohol or a polyvinyl alcohol derivative or a mixture thereof. The present invention also relates to a process for manufacturing the oral pharmaceutical dosage form and to the use in medicine thereof.
EP1586574A1 Medicaments containing betamimetic drugs and a novel anticholinesterase drug Medicaments contain: - (a) a quaternized 2,2-diphenylpropionic acid scopine ester anticholinergic agent (I) and - (b) a beta -mimetic agent (II). - Medicaments contain: - (a) a scopine derivative anticholinergic agent of formula (I); - (b) at least one beta -mimetic agent (II) (optionally in the form of enantiomers, enantiomer mixtures, racemates, solvates or hydrates), and - (c) optionally pharmaceutical auxiliaries. - X- = monovalent anion, preferably chloride, bromide, iodide, sulfate, phosphate, methanesulfonate, nitrate, maleate, acetate, citrate, fumarate, tartrate, oxalate, succinate, benzoate or p-toluenesulfonate. - ACTIVITY - Antiinflammatory; Antiasthmatic. - MECHANISM OF ACTION - Anticholinergic; beta -mimetic.
US20090069437 Compositions for Oral Transmucosal Delivery of Metformin The invention relates to oral transmucosal pharmaceutical compositions comprising metformin or a pharmaceutically acceptable salt thereof, methods of using the compositions to treat various conditions, including diabetes, methods of preparing the compositions, and preparations for use in making the compositions.
US20100093667 Salts of hiv inhibitor compounds The invention is related to salts of anti-viral compounds, compositions containing such salts, and therapeutic methods that include the administration of such salts, as well as to processes and intermediates useful for preparing such salts.
US20120282222 Estrogen receptor ligand and/or interferon beta treatment for neurodegenerative diseases This invention relates generally to novel treatments to prevent neurodegeneration in the central nervous system comprising a therapeutic dosage of an estrogen receptor ligand and/or an immunotherapeutic compound, such as beta-interferon, to ameliorate the effects of the neurodegenerative disease and to stimulate repair.
CA2215834C Dna encoding human papillomavirus type 18 The present invention is directed to DNA molecules encoding purified human papillomavirus type 18 and derivatives thereof.
US20120184495 Targeted nano-photomedicines for photodynamic therapy of cancer The present invention relates to a photosensitizer-containing nanoparticle, comprising a photosensitizer covalently bonded throughout at least a part of said nanoparticle to the nanoparticle matrix material and incorporated therein in a quasi-aggregated state. The present invention further relates to methods for producing the invention nanoparticles, and to methods of killing cancer cells by PDT treatment using the said nanoparticles.
WO2011133039A2 Novel conjugates of cc-1065 analogs and bifunctional linkers This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
US20070270495 Use of Cystine or Cysteine for the Prevention and Treatment of Oxidative Stress Cause by Haemodialysis and of Acute or Chronic Kidney Diseases The invention discloses the use of cystine and/or cysteine for the preparation of oral medicinal products for the prevention and treatment of oxidative stress resulting from haemodialysis treatment in patients suffering from chronic kidney failure as well as for the treatment and prevention of acute or chronic kidney diseases and of End-Stage Renal Disease.
US20080119462 Method for treating vascular hyperpermeable disease The present invention provides a method for treating a vascular hyperpermeable disease (except macular edema), which method comprises administering to a patient in need thereof a vascular adhesion protein-1 (VAP-1) inhibitor in an amount sufficient to treat said patient for said disease.
EP2049530A2 Crystalline nemorubicin hydrochloride This invention relates to a novel crystalline polymorphic form of nemorubicin hydrochloride dihydrate, useful for the preparation of pharmaceutical composition for the treatment of tumors. A process for preparing this novel polymorphic form, named form A, is within the scope of the present invention.
WO2013011461A1 Process for the preparation of asenapine maleate The present invention provides a process for the preparation of asenapine maleate of Formula (I), comprising: intra-molecular cyclization of the intermediate of Formula (II) to obtain the intermediate of Formula (III) using aluminium halide.
WO2013135187A1 Solid dispersion of improved adsorption performance and preparation thereof A solid dispersion of improved adsorption performance and preparation thereof. Specifically, provided in the present invention is the solid dispersion. The solid dispersion comprises (A) serving as an active ingredient and represented by formula A, a compound or a derivative thereof, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and, (B) a hydrophilic macromolecule carrier, where the weight ratio between (A) and (B) is between 1:1 and 1:40. The solid dispersion provided in the present invention significantly increases in vitro dissolution of active ingredients, and greatly increases adsorption of the active ingredients for mammals, thus effectively reducing dosage.
CN1850166A Composition of white mulberry leaf blood-sugar-reducing effective components and preparing method The present invention relates to a mulberry leaf effective component composition for reducing blood sugar and its preparation method. Said mulberry leaf effective component composition contains 20-80% of mulberry leaf polysaccharide and 80-20% of mulberry leaf alkaloid in which 1-deoxynojirimycin content is greater than 50%. Said preparation method includes the following steps: removing impurity, drying, pulverizing to obtain mulberry leaf powder, using organic solvent to make extraction, filtering, removing residue, using hot water to make extraction, filtering, adding ethyl alcohol into filtrate to make its concentration be 40%-80%, filtering to obtain supernatant fluid and precipitate, using cation exchange resin and anion exchange resin to make separation and remove impurity, concentrating and drying so as to obtain mulberry leaf alkaloid.
EP1686999B1 Pyrazole derivatives as inhibitors of receptor tyrosine kinases Compounds of formula (I): and their use in the inhibition of Trk activity are described.
US20110059983 Use of substituted oxindole derivatives for the treatment and prophylaxis of pain The present invention relates to the use of substituted oxindole derivatives of formula I as defined in the claims and description for the treatment or prophylaxis of pain.
CN103110660A Mangiferin-cis-platinum composition and use thereof for treating cancer The invention relates to a mangiferin-cis-platinum composition, a preparation method of the composition and use thereof as a medicine. The cis-platinum aqueous solution is unstable, and the stability of cis-platinum in physiological saline solution is remarkably increased by preparing the mangiferin-cis-platinum composition. In-vitro pharmacological test result shows that the mangiferin-cis-platinum composition is remarkably superior to singly used cis-platinum in effect of inhibiting tumor cell proliferation of liver cancer and the like, so that the use level of cis-platinum is correspondingly reduced, therefore, the side effect is reduced, the patient pain is reduced, and the patient prognosis is improved. The mangiferin-cis-platinum composition can be used for preparing medicines for treating tumors such as liver caner.
EP1867331A1 Triazole derivative and the use thereof The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I) wherein R1a, R1b and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted alkoxy, R3 is a group represented by the formula -NHCOR4, -NHSO2R5, -NHCON(R6a) (R6b), -NHCOOR7 or -CONHR8 wherein R4, R5, R6a, R6b, R7 and R8 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like), ring A is monocyclic aromatic ring optionally further having substituent(s), R1a and R1b are optionally bonded to each other to form an optionally substituted nitrogen-containing non-aromatic heterocycle, or a salt thereof or a prodrug thereof. The thrombin receptor antagonist of the present invention has a thrombin receptor (particularly PAR-1) antagonistic action and is useful for the prophylaxis or treatment of PAR-1 mediated pathological condition or disease.
US20090270513 3,5-dihydroxy-2,4-cyclohexadienones and their derivatives, dietary compositions and fortified food containing them and their uses The present invention refers especially to 3,5-dihydroxy-2,4-cyclohexadienones of the general formula (I) wherein R1 and R2 are independently from each other C1-6-alkyl, C2-6-alkenyl or x-oxo-Cx-alkyl with x being an integer from 1 to 6, preferably R1 and R2 are independently from each other C2-6-alkenyl or y-oxo-Cy-alkyl with y being an integer from 2 to 5, and wherein R3 and R4 are independently from each other hydroxy, C1-6-alkyl, C2-6-alkenyl or x-oxo-Cx- alkyl with x being an integer from 1 to 6, preferably R3 and R4 are independently from each other hydroxy or y-oxo-Cy-alkyl with y being an integer from 2 to 5, for use as mood balancing agents and stress relievers, as well as to dietary compositions and fortified food/feed/beverages containing such 3,5-dihydroxy-2,4-cyclohexadienones of the general formula (I), and their uses.
US7105554 Benzylidene thiazolidinediones and their use as antimycotic agents A compound of formula I or a salt thereof wherein, A is O or S, X and Y independently represent O, CH2 and may be the same or different, Q is (CH2)m—CH(R1)-(CH2)n, R is OR6, NHR8, R1 is hydrogen, or optionally substituted alkyl, R2 and R3 are independently hydrogen, or specific substituents, provided that R2 and R3 are not both H, and R4 and R5 are hydrogen or specific substituents, m is 0–3; n is 0–2; are useful in the treatment of fungal infections.
WO2006081072A1 Antagonists of the mglu receptor and uses thereof The present invention discloses compounds of general formula (I) wherein X1-X4 and R1-R3 are as defined in the description. The present invention also discloses methods of treatment for pain, neurodegeneration and convulsive states in a host mammal in need thereof, and pharmaceutical compositions including those compounds.
US7812036 Androgens The compounds of the subject invention have a structure according to formula I: wherein each of the substituents is given the definition as set forth in the specification and claims, or a salt or hydrate form thereof.
CN1726918A Method for preparing Meloxicam freeze-dry powder A freeze-dried powder injection of meloxicam features that the clear solution before freeze-dying contains proportionally meloxicam, hydroxypropyl-beta-cyclodextrin, cosolvent, dissolving promoter, osmotic pressure regulator and pH regulator. Its preparing process is also disclosed.
CA2273823C Polypeptides encoded by a human lipase-like gene, compositions and methods Lipoprotein Lipase like polypeptides, nucleic acids encoding said polypeptides, antisense sequences, and antibodies to said polypeptides are disclosed. Also disclosed are methods for the preparation of said polypeptides in a recombinant system and for the use of said polypeptides to screen for agonists and or antagonists of said polypeptides. Also disclosed are methods and compositions for the treatment of disorders of lipid metabolism.
CN101904821A Quercetin nano freeze-dried powder and preparation method thereof The invention relates to quercetin nano freeze-dried powder and a preparation method thereof. The freeze-dried powder consists of quercetin, surfactant and freeze-drying protectant; and after the freeze-dried powder is dispersed in water, the particle size of the freeze-dried powder is 100 to 300 nano meters. The quercetin nano freeze-dried powder provided by the invention has the advantages that: the composition is simple; auxiliary materials are selected from common medicinal auxiliary materials; the preparation method is economic and reliable; industrial production can be realized; and industrial production is possible. In the invention, quercetin nano freeze-dried powder is prepared by a freeze-drying method, so the storage stability of medicaments is improved, and nano solid preparations such as pills, granules, tablets and capsules can be prepared through further processing.
WO2008034580A3 Uses of cripowellins and the derivatives thereof for the treatment of tumor diseases The invention relates to the use of cripowellins and the derivatives thereof for producing medicaments utilized for treating tumor diseases.
EP1834959A2 Tert-butyl-substituted aromatic steroids having cytoprotective activity The present invention is directed to modified, hydroxy-bearing aromatic ring structures having cytoprotective activity. More specifically, in a first embodiment the present invention is directed to phenolic compounds, and in particular steriods (eg., estrogens), hydrophobic substituent is attached to the hydroxy-substituted A-ring thereof. The present invention is further directed to a process for conferring cytoprotection to a population of cells involving the administration of the compound.
EP2524692A1 Anti-inflammatory analgesic adhesive patch for external use An external patch containing diclofenac hydroxyethylpyrrolidine prepared by laminating an adhesive layer on a backing, wherein said adhesive layer is characterized by comprising 5-50% by weight of styrene·isoprene·styrene block copolymer, 20-50% by weight of a tackifier resin, 5-70% by weight of a softening agent, and 0.5-20% by weight of one or more solubilizers selected from N-methyl-2-pyrrolidone, propylene glycol and dimethyl sulfoxide as essential ingredients, and 0.5-20% by weight of diclofenac hydroxyethylpyrrolidine as an active ingredient. The patch has excellent transdermal absorption, less skin-irritation and excellent stability of the drug.
CN101829106B Application of diallyl propyl flavonolignan in preparation of medicament for curing hepatitis B The invention relates to an application of diallyl propyl flavonolignan in preparation a medicament for curing hepatitis B, in particular to application of a flavonolignan or pharmaceutically acceptable salts thereof in preparation of the medicament for curing the hepatitis B by clearing hepatitis B e-antigen and inhibiting HBV DNA replication. The flavonolignan has hepatitis B virus e-antigen (HBeAg) inhibiting activities, and has the inhibition strength higher than a positive control first-line medicament, namely lamivudine and alpha-interferon, at a low concentration of 20 mu g/ml; simultaneously, at the concentration of 5 mu g/ml, the compound has an inhibition rate of the HBV DNA of over 70 percent; and therefore, the flavonolignan can be expected for preparing the medicament for curing the hepatitis B virus infection diseases by clearing the hepatitis B e-antigen and inhibiting the HBV DNA replication.
CN103751174A Application of schisandra chinensis monomer compound in preparation of drugs for prevention and treatment of hepatotoxicity caused by acetaminophen The invention discloses an application of a schisandra chinensis monomer compound in preparation of drugs for prevention and treatment of hepatotoxicity caused by acetaminophen (APAP), wherein the schisandra chinensis monomer compound is deoxyschizandrin, schisandrin C, schisandrin or schisantherin a. Experiment results show that: with the schisandra chinensis monomer compound, the ALT content and the AST content in the APAP-induced liver injury animal model can be significantly reduced, consumption of glutathione in liver cells can be inhibited, the liver cell necrosis degree can be effectively improved, and the schisandra chinensis monomer compound provides significant treatment and protection effects for hepatotoxicity symptoms caused by APAP.
CN102850220A Sea asparagus ferulic acid ester compound as well as preparation method and application of compound The invention belongs to the field of marine biotechnology, and discloses a sea asparagus ferulic acid ester compound as well as a preparation method and application of the compound. The sea asparagus ferulic acid ester compound is ferulic acid pentadecane ester which has the structural formula shown in a formula (I). The ferulic acid pentadecane ester separated out from sea asparagus is the compound obtained from natural resource for the first time, and has high oxidative activity and strong activity for removing free radicals, thus the sea asparagus ferulic acid ester compound can be used as a symbolic antioxidant active ingredient and a natural free-radical scavenger in the sea asparagus.
CA2184077C Nasal and ocular administration of ketamine to manage pain and for detoxification The present invention relates to the management of chronic pain without requiring administration of narcotics, and to self-management of pain on an outpatient basis. The invention further relates to facilitating detoxification and treatment of substance addiction. Accordingly, the present invention is broadly directed to a method for treating pain in a subject comprising administering via a nasal route a dose of ketamine effective to alleviate pain to a subject suffering from pain. The invention is further directed to a method for facilitating detoxification and treating substance addiction in a subject comprising administering via a nasal route a dose of ketamine effective to facilitate detoxification or treat substance addiction. In a further embodiment, the present invention provides for pulmonary administration of ketamine by inhalation. Nasal administration of ketamine advantageously allows for patient self administration of the drug, which provides for pain management or treatment of a substance addiction on an outpatient basis. Moreover, ketamine administration in nasal sprays and inhalers are generally socially acceptable. In a specific example, a patient suffering from intractable bladder pain controlled breakthrough pain by nasal administration of about 16 mg to about 32 mg of ketamine per dose.
US20090005388 3-Heteroaryl-3,9-Diazabicyclo[3.3.1]Nonane Derivatives as Nicotinic Acetylcholine Receptor Agonists This invention relates to novel 3,9-diazabicyclo[3.3.1]nonane derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
CA2200760C Aqueous compositions containing ciprofloxacine, and related use and process Aqueous compositions containing ciprofloxacine and corresponding use and process, said composition comprising from 0.12-0.6 g/ml of chlorohydrate monohydrate of ciprofloxacine (equivalent to 0.1-0.5% of free base); 0.5-3.0 g/ml of a buffer system capable of maintaining the pH between 4 and 5; 0.05-0.3 g/ml of a non ionic surface--active agent; from 0.5-2.0 g/ml of a thickening agent; and the rest to 100 ml of water.
WO2014143592A1 Inhibition of neovascularization by inhibition of prostanoid ip receptors There are provided inter alia methods and compounds useful for decreasing choroidal neovascularization in a subject in need thereof.
US20070155713 Nitrogen-containing heterocyclic compounds and use thereof A pharmaceutical composition comprising, as an active ingredient, the compounds represented by formula (I) (wherein all of the symbols have the same meanings as defined in specification.), salts thereof, solvates thereof, or prodrugs thereof. The compounds represented by formula (I) are used for prevention and/or treatment of various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, chronic rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis and the like), immunologic diseases (treatment of autoimmune diseases, transplant rejection, immunosuppression, psoriasis, multiple sclerosis and the like), human immunodeficiency virus infection (acquired immunodeficiency syndrome and the like), allergic diseases (atopic dermatitis, nettle rash, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis and the like), suppression of ischemia-reperfusion injury, acute respiratory distress syndrome, shock accompanied by bacterial infection, diabetes mellitus, or metastasis and the like.
CN101905025A Preparation method for protective agent of intestinal mucosal barrier The invention discloses a preparation method for a protective agent of an intestinal mucosal barrier. Butyric acid is absorbed or bonded on a silica gel surface or in a hole by using silica gel; and after being stirred and mixed, synthesized silica gel loading butyric acid and stearate are dried and pulverized. Because of having the characteristics of high surface activity, microporous structure and large specific surface area, the silica gel has good biocompatibility and intestinal mucosal affinity and a function of controlling slow release for the loaded butyric acid. In addition, the stearate reacts with the silica gel loading butyric acid in the process of stirring and mixing to generate byterate, and the stearate has an envelope function to add the storage stability of a product. The protective agent of the intestinal mucosal barrier can repair and protect intestinal epithelial cells, maintain the normal barrier of the intestinal mucosa and beneficial microorganism of the intestinal mucosa, and enhance health level of animals, daily gain and feed conversion efficiency.
WO2013184698A1 Solid forms of an antiviral compound Amorphous and crystalline solid forms of the anti-HCV compound (1-{3-[6-(9,9-difluoro-7-{2-[5-(2-methoxycarbonylamino-3-methyl-butyryl)-5-aza-spiro[2.4]hept-6-yl]-3H-imidazol-4-yl}-9H-fluoren-2-yl)-1H- benzoimidazol-2-yl]-2-aza-bicyclo[2.2.1]heptane-2-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester (Compound I) were prepared and characterized in the solid state: (Compound (I)). Also provided are processes of manufacture and methods of using the amorphous and crystalline forms.
US7101894 Administering quinoline derivative for therapy of Cytomegalovirus infections in human pathogen Methods for treating CMV or a CMV-related disease are provided that use compounds having the formula: wherein Ar is a substituted or unsubstituted 5–14 membered heteroaryl group having from 1 to 5 heteroatoms as ring members; R1 is selected from the group consisting of substituted or unsubstituted aryl(C1–C4)alkyl, heteroaryl(C1–C4)alkyl, —C(O)R11, and —C(O)NR11R12, wherein each R11 and R12 independently is substituted or unsubstituted aryl, substituted or unsubstituted aryl(C1–C4)alkyl, substituted or unsubstituted (C4–C8)cycloalkyl(C1–C4)alkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaryl(C1–C4)alkyl and substituted or unsubstituted hetero(C4–C8)cycloalkyl(C1–C4)alkyl; R2 is H or (C1–C8)alkyl; and ZN is a substituted or unsubstituted hetero(C6–C10)bicycloalkyl group.
US20090012091 Oximide derivatives and their therapeutical application The present invention relates to a compound represented as the following Formula (I) and a pharmaceutical composition thereof wherein all substituents are as defined in the specification; and also relates to a method for treating or lessening the severity of a disease or a condition, comprising administering said compound or said pharmaceutical composition.
CN102018799A India madder root-twotooth achyranthes root blood-activating and stasis-dissolving wine and preparation method thereof In the formula, India madder root has the effects of cooling blood, activating blood, dissolving stasis and relieving pain; twotooth achyranthes root has the effects of activating blood, dissolving stasis and removing obstruction in channels to relieve pain; rhubarb has the effects of clearing away heat and toxic material, dissolving stasis, eliminating swelling and relieving pain; bitter orange has the effect of regulating the flow of qi; dahurian angelica root has the effects of eliminating stagnation, eliminating swelling and relieving pain; and liquor has the effects of activating blood and promoting the circulation of qi. Wine prepared from the raw materials has the effects of clearing away heat, cooling blood, activating blood, dissolving stasis, eliminating swelling and relieving pain and is used at the early stage of closed injury. The wine is smeared on a wounded part twice a day.
CN1899281A Use of chlorogenic acid in preparing medicine for improving immunity function The present invention discloses the use of chlorogenic acid in preparing medicine for raising immunological function alone or together with other medicine component.
US20120237550 Maintaining Antibody-Binding Activity Of Immunosuppressant Drug Conjugates Methods and reagents are disclosed for maintaining the antibody-binding activity of a conjugate of an immunosuppressant drug and a conjugative moiety. The method comprises combining with the conjugate an effective amount of a chelating agent. Compositions include in an aqueous medium (i) a conjugate of an immunosuppressant drug and a conjugative moiety and (ii) a chelating agent in an amount effective to maintain an antibody-binding activity of the conjugate of the immunosuppressant drug and the conjugative moiety. The compositions may be employed in assays for the determination of analytes that include immunosuppressant drug analytes and antibodies for an immunosuppressant drug.
US20110098268 Spirocyclic compounds The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
CN103012338A Nepeta lactone parabromobenzoate and preparation process and application thereof The invention discloses a nepeta lactone parabromobenzoate and a preparation process and application thereof. The nepeta lactone parabromobenzoate has the molecular formula of C17H17BrO4, the melting point of 179 to 181 DEG C and the specific rotation shown in the FORMULA (referred to the Specification). The invention further discloses an extracting method of the nepeta lactone parabromobenzoate and application of the nepeta lactone parabromobenzoate to preparation of an anti-influenza virus resisting medicine.
CN1927225A Cleaning agent for treating dermatopathy The invention discloses a cleaning agent for treating skin diseases, which comprises white alum, magnesium sulfate and zinc sulphate and the preparing process comprises disintegrating the raw materials. The agent can be used for treating bedsore, folliculitis, eczema, lower limb ulcer and acne.
WO2013026874A1 Cdk9 inhibitors in the treatment of midline carcinoma The present invention relates to a CDK9 inhibitor, especially a selective CDK9 inhibitor, for use in treating, ameliorating and/or preventing midline carcinoma. Also corresponding methods for treating, preventing or ameliorating midline carcinoma are subject of the present invention. Preferably, NUT midline carcinoma is treated with the CDK9 inhibitors in accordance with the present invention.
EP1156827B1 USE OF COMPOSITIONS COMPRISING CldC AS RADIOSENSITIZERS IN THE TREATMENT OF NEOPLASTIC DISEASES The present invention is related to agents useful in the treatment of tumors by radiation by sensitizing tumor cells toward the radiation. The agents of the invention can perform selective tumor radiosensitization and be involved in tumor directed hypomethylation. The agents of the invention include (a) 5-chloro-2'-deoxycytidine (CldC) administered without a cytidine deaminase inhibitor, (b) CldC administered with a cytidine deaminase inhibitor, (c) CldC and 4-N-methylamino 5-fluoro-2'-deoxycyxtidine (4-N-methylamino FdC), or (d) CldC and 4-N-methylamino FdC coadministered with a cytidine deaminase inhibitor. The cytidine deaminase inhibitor can be tetrahydrouridine or Zebularine. Within the scope of the invention are methods of treating tumors by administering the agents of the present invention without the need of other modulators of metabolism. Another aspect of the invention is a method of hypomethylating a gene silenced in a tumor of a subject by administering the agents of the invention to the subject to reduce the aggressiveness of the tumor, the metastatic propensity of the tumor, the genetic instability of the tumor, and/or the resistance of the tumor to drug or radiation treatment. An additional aspect of the invention is a method of protecting normal tissues during a radiation treatment of a tumor in a subject by administering the agents of the invention to the subject before or during the radiation treatment. The agents of the invention can be combined with new sources or new schedules of radiation, and new categories of tumors can also be treated with the agents of the invention.
CN103110636A Paracetamol and caffeine dropping pill and preparation method thereof The invention relates to a paracetamol and caffeine dropping pill and a preparation method thereof. The paracetamol and caffeine dropping pill comprises an active ingredient clathrate compound, a matrix and a stabilizer, wherein the active ingredient clathrate compound comprises active ingredients and clathrate material; the active ingredients consist of paracetamol and caffeine in ratio by weight of 1:0.13; the clathrate material includes alpha-cyclodextrin, beta-cyclodextrin and hydroxy beta-cyclodextrin; and the matrix is selected from the mixtures each including two of polyethylene glycol 6000, polyethylene glycol 4000, polyoxyethylene stearate, sodium stearate, glycerin gelatine, poloxamer, stearic acid and the like. The weight ratio of the active ingredients and the clathrate material is (3:2)-(2:3). The paracetamol and caffeine dropping pill disclosed by the invention has the advantages of good roundness, fast drug digestion and high bioavailability.
CN101926795A Medicinal composition for treating hyperur icemia The invention relates to a medicinal composition for treating hyperur icemia. The composition consists of febuxostat crystals, benzbromarone and a pharmaceutically acceptable medicinal carrier of which the ratio of part by weight is 1:1-8:0.05-100. Pharmacological experimental researches on the medicinal composition show that the medicinal composition has obvious synergetic effect, can quickly reduce the concentration of uric acid in blood serum and obviously improves hyperur icemia treatment effect. Particularly, when the ratio of the febuxostat crystals to the benzbromarone is 1 to 2, the inhibiting effect is improved by over 60 percent; and when the ratio of the febuxostat crystals to the benzbromarone is 1 to 4, the inhibiting effect is improved by over 300 percent.
CA2124932C Sex steroid activity inhibitors Inhibitors of sex steroid activity, for example those having general structure may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.
CN101984999A Healing powder The invention discloses a method for manufacturing healing powder. The invention is implemented by the following technical scheme that the method comprises the following steps of: slightly frying pigeon excrement for 1 to 2 hours till browning, frying fish glue C swimming bladder and clam meal till browning, baking white stiff silkworm and lichen by using a mud tile, grinding the materials into fine powder of 500 meshes together, adding bovine calculus powder into the fine powder, and stirring the mixture for 5 minutes to obtain a powder product. The healing powder manufactured by using the method can heal the wound in one day.
US7838540 3-aminocarbonyl, 6-phenyl substituted pyridine-1-oxides as p38 kinase inhibitors Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
WO2010026177A1 1,4-diaza-bicyclo [3.2.2] nonyl pyridine derivatives as nicotinic and monoamine receptor modulators This invention relates to novel 1, 4-diaza-bicyclo [3.2.2] nonyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
CN1602862A Application of leflunomide in the preparation process of anti SARS virus medicine The invention provides application of leflunomide to preparing anti-SARS virus drugs. It is testified that the active metabolite of the leflunomide-furosemide has the effects of resisting SARS viruses and protecting the infected cells through the anti-SARS virus screening test by the national drug screening center, therefore the leflunomide and its active metabolite-furosemide can be applied to prepare the anti-SARS virus drugs.
WO2008065666A3 Uses of incensole, incensole acetate and derivatives thereof The invention relates to the use of incensole, incensole acetate, and derivatives thereof, for the treatment, prevention or amelioration of diseases or conditions such as: inflammatory-associated conditions; a disease or condition where neuroprotection is required; a disease or condition selected from depression, anxiety, obsessive compulsive behaviors, deterioration in cognitive function, and deterioration in neurobehavioral function. The invention further relates to pharmaceutical compositions and method of treatment, prevention or amelioration of the above-mentioned diseases or conditions.
US8524694 Aminoalkylsterol compounds with antitumoral and neuroprotective activity Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.
US20130041019 SDF-1 Binding Nucleic Acids The present invention is related to an L nucleic acid that binds to an SDF-1.
US8476416 comprises a dinucleotide analog that includes a non-naturally occurring pyrimidine base; for treating autoimmune disorders, such as autoimmune asthma; allergies The invention relates to the therapeutic use of oligonucleotides or oligonucleotide analogs as immunostimulatory agents in immunotherapy applications. The invention provides methods for enhancing the immune response caused by immunostimulatory oligonucleotide compounds.
CN103393713A Hyaluronic acid and application of salt thereof in preparing medicines for treating constipation The invention relates to the field of medicines, and discloses hyaluronic acid and an application of salt thereof in preparing medicines for treating constipation. The invention further provides a pharmaceutical composition or a combined pharmaceutical box for loosening the bowel to relieve constipation. The pharmaceutical composition or the combined pharmaceutical box comprises hyaluronic acid and medicines for adjusting intestinal flora or dietary fiber. Preferably, the medicines for adjusting intestinal flora are selected from xylooligosaccharide, fructo-oligosaccharide, galactooligosaccharide, soybean oligosaccharide or isomaltooligosacharide. The hyaluronic acid disclosed by the invention and the medicines for adjusting intestinal flora or dietary fiber are applied at the same time, so that the hyaluronic acid is suitable for treating constipation for patients with cardiovascular diseases.
CN101669926A Liquid preparation for dosing nasal cavities and method for making the same The invention relates to a liquid preparation for dosing nasal cavities, which comprises 0.1 to 25 g/100 mL of rupatadine and 0.5 to 30 g/100 mL of cyclodextrin compound. The invention also relates toa method for making the liquid preparation. The liquid preparation of the invention has the characteristics of convenient use, high patient compliance and rapid absorption speed after dosing.
CN103550756A Paste for treating acne The invention discloses paste for treating acne. The paste for treating acnes comprises the following components in parts by weight: 8-15 parts of crystal soda powder, 3-5 parts of camphor, 2-4 parts of borneol, 4-8 parts of sulfur, 1-3 parts of almond, 0.5-1 part of interleukin, 10-20 parts of castor oil, 4-8 parts of Chinese angelica and 30-60 parts of vaseline. Compared with the prior art, paste for treating acnes has the effects of relieving internal heat or fever, diminishing inflammation, dredging sebaceous gland catheters, accelerating the healing of wounds and the like and the beneficial effects of improving the resistance of skin, fading pigment, enabling the skin to physiologically whiten and be fine and smooth, reducing relapse and the like.
CN102973568A Preparation method of liposome of medicine composition of ceftriaxone sodium and sulbactam sodium The invention relates to a preparation method of liposome of a medicine composition of ceftriaxone sodium and sulbactam sodium. According to the method, the liposome is prepared in a combining form of medicines, and the specification proportion of the ceftriaxone sodium to the sulbactam sodium is equal to (1-4):1. The preparation method comprises the following main steps of: preparing blank liposome from phospholipid and cholesterol, preparing the liposome from the ceftriaxone sodium and the sulbactam sodium which are respectively subjected to passive loading, and performing freeze drying on the prepared liposome to obtain a finished product; or dissolving the ceftriaxone sodium and the sulbactam sodium in phosphate buffer with the pH ranging from 6.0 to 6.5, and adding phospholipid cholesterol and a freeze-dried support agent to the solution in an active loading manner to prepare a freeze-drying preparation of the liposome.
US7388006 Non-steroidal progesting The present invention relates to non-steroidal progestins of the general formula (I) wherein R1 and R2 are independently of each other —H or —F, R3 is —CH3 or —CF3, and Ar is or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.
CN102379914A Pharmaceutical composition for treating Alzheimer disease (AD), and preparation method and application thereof The invention discloses a composition of extractives of hedysarum polysaccharide and rhodiola rosea, a preparation method thereof and application of compatibility of the same in preparing medicines for treating AD. The compatibility of the extractives of hedysarum polysaccharide and rhodiola rosea in the invention can remarkably protect SH-SY5Y cells from being damaged by Abeta25-35 and increase the viability of the SH-SY5Y cells; according to results of Morris water maze tests, it is revealed that the extractives of hedysarum polysaccharide and rhodiola rosea can substantially enhance learning and memory ability and cognitive impairment of AD model rats; according to results of further detection, the compatibility of the extractives of hedysarum polysaccharide and rhodiola rosea enables the level of glucose metabolism in brains of the AD model rats to recover, which indicates that the compatibility of the extractives of hedysarum polysaccharide and rhodiola rosea has the effect of treating AD and has a remarkable effect.
CN101817819A 5-alkoxy-tetrazo[1,5-a]qualone derivative and pharmaceutically acceptable salt thereof serving as antidepressants The invention relates to novel 5-alkoxy-tetrazo[1,5-a]qualone compounds, which are represented by a general formula I, and an addition salt formed by the compound and pharmaceutically acceptable acid. The invention also relates to use of the compounds and the addition salt formed by the compounds and the pharmaceutically acceptable acid as antidepressants.
CA2468916C A stable oxaliplatin solution formulation The present invention relates to novel stable solution formulations comprising oxaliplatin, an effective stabilizing amount of lactic acid and/or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. A method for manufacturing such formulations ready for administration and their use in the antitumor therapy are also within the scope of the invention.
WO2014135107A1 Novel nucleoside phosphoramidate compound and use thereof Provided are a novel nucleoside phosphoramidate compound, stereoisomer, salt, hydrate, solvate or crystal thereof for treating flaviviridae virus, in particular a hepatitis C virus infection. Also provided are a pharmaceutical composition containing the compound, stereoisomer, salt, hydrate, solvate or crystal thereof, and uses of the compound and composition for treating the flaviviridae virus, in particular the hepatitis C virus infection. The compound has a good anti-HCV effect.
CN103585195A Application of Lepisorus clathratus Ching extract in preparation of anticancer drugs The invention discloses new application of a Lepisorus clathratus Ching extract in preparation of anticancer drugs. The Lepisorus clathratus Ching extract is prepared by: taking Lepisorus clathratus Ching as a raw material, conducting extraction with 30%-90% ethanol, and carrying out macroporous adsorption resin purification twice. The Lepisorus clathratus Ching extract provided by the invention is of great significance in preparation of anticancer drugs, especially anti-liver cancer, lung cancer and gastric cancer drugs.
WO2007056851A1 Compositions and methods for enhancing ovulation inducing agents The invention relates to compositions, conjugates, and methods for the prevention and/or treatment of infertility, in particular unexplained infertility, comprising a therapeutically effective amount of an ovulation inducing agent and an ovulatory function enhancing agent. In aspects of the invention, the ovulation inducing agent is clomiphene or clomiphene citrate and the ovulatory function enhancing agent is N-acetylcysteine.
EP1411984B1 Combination medicament for treatment of neoplastic diseases which contains cyanoguanidine ikk inhibitors and a second anti-neoplastic drug Pharmaceutical composition comprising, as a first anti-neoplastic drug, cyanoguanidine IKK inhibitors, and in particular compounds of formula (I) wherein n is 0, 1 or 2; each R independently represents halogen, trifluoromethyl, hydroxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxycarbonyl, nitro, sulfo, cyano, amino or carboxy groups; Q is a straight or branched, saturated or unsaturated C4-20 divalent hydrocarbon radical; X is a bond, amino, O, S, carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino; A is di-( C1-4 alkoxy)phospinoyloxy, C1-4 -alkoxycarbonyl, C1-4 alkoxycarbonylamino, C3-12 carbocyclic ring or C3-12 heterocarbocyclic ring optionally subtituted with one or more R1; R1 being independently selected from the group consisting of halogen, trifluoromethyl, hydroxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxycarbonyl, nitro, cyano, amino, sulfo, carboxy, carboxamido, sulfamoyl or C1-4 hydroxyalkyl; in combination with a second anti-neoplastic drug are provided.
US7109225 Substituted oxazole derivatives The present invention relates to compounds of formula (I) wherein R1 to R8 and n are as defined in the description and claims, and pharmaceutically acceptable salts and esters thereof. The compounds are useful for the treatment of diseases such as diabetes.
WO2012107905A1 Composition for use in the treatment of menopause problems/disorders and in the treatment of general aging of the organism. The invention concerns a composition for the prevention and/or the treatment of menopausal syndrome and/or of aging comprising an association of an equolbased active metabolite of daidzein with resveratrol, in an edible carrier or excipient. The invention composition may be in the form of a nutraceutical or pharmaceutical preparation.
US20100324141 High purity 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides and methods of use thereof A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]-propanamides and their salts with pharmaceutically acceptable acids with a high degree of purity, i.e. with a content of dibenzyl derivatives impurities lower than 0.03% by weight. The process is carried out by submitting a Schiff base intermediate to a reduction reaction with a reducing agent in an amount of organic solvent to allow the formation (and presence during a substantial portion of the reduction reaction) of a suspension of the Schiff base.
CN102860993A Hydrochloric acid vilazodone quick-release tablet and preparation method thereof The invention discloses a hydrochloric acid vilazodone quick-release tablet and a preparation method thereof. The hydrochloric acid vilazodone quick-release tablet comprises the follow components by mass: 2-12% of hydrochloric acid vilazodone, 28-45% of lactose, 40-60% of microcrystalline cellulose, 0.5-3% of lubricants and 1-5% of coating materials. The lubricants include magnesium stearate and colloidal condition silica or one of the magnesium stearate and the colloidal condition silica. The hydrochloric acid vilazodone quick-release tablet is prepared through the following steps: evenly mixing the hydrochloric acid vilazodone, the lactose, the microcrystalline cellulose and the lubricants according to proportion of a formula, detecting whether content uniformity is qualified, and pressing the mixture into tablets when the content uniformity is qualified. The hydrochloric acid vilazodone quick-release tablet has special requirements for grain size of the hydrochloric acid vilazodone, and the preparation process saves time and labor, reduces energy consumption and improves production efficiency. Disintegration speed of medicines is fastened, the dissolving-out time is obviously less than that of a prescription which has no limitation on the grain size of the hydrochloric acid vilazodone, and simultaneously the process which directly performs mixing tabletting greatly improves stability of the medicines in preparations.
CN101032517A Medicine for curing dermatophytosis The present invention discloses one kind of tinea pedes treating medicine, and belongs to the field of medicine technology. The tinea pedes treating medicine is prepared with benzoic acid 6-15 weight portions, salicylic acid 3-9 weight portions, calamine 50-55 weight portions, zinc oxide 26-36 weight portions, mint oil 0.8-1.2 weight portions, camphor 1.5-2.5 weight portions, and boric acid 4-6 weight portions. It has the functions of killing fungi, stopping itching, astringing, diminishing inflammation, etc.
WO2012167018A1 Targeted delivery of retinoid compounds to the sebaceous glands Disclosed herein are topical dermal compositions comprising particles, wherein the particles comprise a) a biodegradable polymer, and b) a retinoid selected from the group consisting of: (I) and (II), or a pharmaceutically acceptable salt thereof, wherein the particles have an average diameter between 0.1 μιτι and 10 μιτι, and wherein the variables are as defined in the specification. The compositions are useful for treating a condition associated with excess sebum production.
EP2447272A1 2'-Fluoro-2'-deoxytetrahydrouridines as cytidine deaminase inhibitors The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.
US8247377 Non-steroidal glucocorticoid inhibitors and their use in treating inflammation, allergy and auto-immune conditions The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation, allergy and/or autoimmune conditions.
EP1326592B1 Use of polyethylene glycol ( peg ) for the manufacture of a medicament for the treatment of constipation Overnight relief of constipation symptoms is achieved, and control of bowel function is enhanced by oral administration of an effective or sufficient amount of a composition comprising polyethylene glycol (PEG), preferably dispersed and or dissolved in an aqueous medium. The PEG compositions used for the present invention are preferably substantially free of ancillary electrolytes.
EP1937665A1 4- (4-BROMO-2-FLUOROANILINO) -6-METHOXY-7- (l-METHYLPIPERIDIN-4 -YLMETHOXY) QUINAZOLINE MONOHYDRATE The present invention relates to a ZD6474 monohydrate, to processes for the preparation of a ZD6474 monohydrate, to pharmaceutical compositions comprising a ZD6474 monohydrate as the active ingredient, to the use of a ZD6474 monohydrate in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to the use of a ZD6474 monohydrate in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability, such as cancer, in warm-blooded animals such as humans.
US20120282267 Cathepsin inhibitors for the treatment of bone cancer and bone cancer pain The present invention is directed to methods of using compounds that are inhibitors of cysteine proteases, in particular, of both cathepsins S and K and optionally further cathepsins B and/or L in treating bone cancer. The present invention is directed to pharmaceutical compositions comprising these compounds for treating bone cancer and bone cancer pain, especially the pain associated with metastasis. A single compound can be used to ameliorate the pain, the injury to bone, while also reducing tumor growth, the risk of metastasis and/or invasiveness of the cancer.
US20110038943 Milkweed seed oil administered to animals Milkweed seed oil administered to an animal improves the health of the animal. This improvement is evidenced by the positive change in the analytical results of blood tests for cholesterol after the animal has been administered an effective amount of milkweed seed oil as compared to the blood test results of the animal before the milkweed seed oil was administered.
EP1976496A1 Overall therapeutic approach in the treatment of neurodegenerative diseases The present invention relates to a pharmaceutical product and to its use in the prevention and treatment of neurodegenerative diseases in humans. The method is based on the action of pantethine-derived substances which have demonstrated an up until now unsuspected effectiveness in protecting the integrity of the blood-brain barrier. By virtue of its method that can be generalized to many neurodegenerative diseases, the present invention significantly differentiates from the conventional therapeutic approaches which associate a treatment for each pathogenic origin.
US20110172171 Taurine or taurine-like substances for the prevention of brain oedema The present invention relates to taurine or taurine-like substances for the prevention of brain oedema, particularly brain intramyelinic oedema and more particularly brain intramyelinic oedema induced by an anti-convulsive drug such as vigabatrin. The invention relates to a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis for the prevention of brain oedema.
US20110124721 Methods of treating traumatic brain injury by administering baicalein preparation The invention provides a novel medical use of Baicalein, and in particular, a use of baicalein in the preparation of a pharmaceutical composition useful for treating traumatic brain injury. The baicalein pharmaceutical composition in this invention includes a treating effective amount of baicalein and a suitable pharmaceutically acceptable excipient or carrier. The baicalein pharmaceutical composition is applicable for improving the behaviour function deficit in traumatic brain injury, reducing the contusion volume of traumatic brain injury, improving the brain neuronal degeneration in traumatic brain injury, reducing proinflammatory cytokines such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6) or other relative inflammation factor induced in traumatic brain injury.
US20090075910 Deuterium-enriched fondaparinux The present application describes deuterium-enriched fondaparinux, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2005034650A1 Weight-loss supplement A weight-loss supplement comprising a satiety-promoting ingredient that includes a mixture of dietary fibers comprising glucomannan and a gum and; a thermogenic ingredient selected from the group consisting of caffeine, catechin-polyphenol and combinations thereof.
CN103142634A Spirulina phatensis polysaccharide and cynomorium songaricum polysaccharide preparation and manufacture method thereof and application thereof The invention provides a preparation containing spirulina phatensis polysaccharide and cynomorium songaricum polysaccharide and manufacture method thereof and application. The preparation is prepared by adding a stabilizing agent, acidity regulator, a flavoring agent and preservative after spirulina phatenisis polysaccharide and cynomorium songaricum polysaccharide are dissolved in distilled water. The formula is 40mg/ml-260mg/ml of the spirulina phatensis, 60mg/ml-300mg/ml of the cynomorium songaricum polysaccharide, 6mg/ml-62mg/ml of the stabilizing agent, 0.1mg/ml-5mg/ml of the acidity regulator, 0.1mg/ml-15mg/ml of the flavoring agent and 0.1mg/ml-0.3mg/ml of the preservative. The spirulina phatenisis polysaccharide is free of harmful smell. The acidity regular and the flavoring agent are added so that smell and taste of the preparation can be improved and therefore the preparation is good in taste and stability. Oral liquid is prepared by the spirulina phatensis polysaccharide and the cynomorium songaricum polysaccharide so that absorption to polysaccharide of a human body is improved, synergy effect of the two kinds of polysaccharide is improved, and the preparation has the functions of promoting protein synthesis, anti-fatigue and enhancing body immunity capacity. The preparation is capable of obviously improving inhibition ratio of cancer cells and is suitable for cancer patients.
US20060251708 Coenzyme q10 containing proliposome and preparation thereof A coenzyme Q10 and ceramide-containing preliposome, and pharmaceutical preparations and cosmetics containing the same. The preliposome can further comprise other lipid components. A granular and lyophilized solid-preparation is produced by lyophilization or spray drying. Then, the coenzyme Q10-containing proliposome is obtained by adding water in the said solid-preparation and shaking. Transdermal absorption of coenzyme is improved together with the effect of coenzyme Q10 in cosmetics and the stability of coenzyme Q10 and liposome, which facilitate the formulation of cosmetics.
CN101862293B Doxycycline hydrochloride oil turbid liquor, preparation method and application thereof The invention discloses doxycycline hydrochloride oil turbid liquor, a preparation method and application thereof. The doxycycline hydrochloride oil turbid liquor of the invention is obtained through preparing 50 to 300g of doxycycline hydrochloride raw medicine, 1 to 50g of suspending aids, 1 to 30g of surface active agents, 0.1 to 2g of oxidation inhibitors and a proper amount of oil into the oil turbid liquor with the volume amount of 1L. The doxycycline hydrochloride oil turbid liquor of the invention is prepared by a dispersing method, has the advantages of high stability, prolonged absorption time, delayed peak reaching time, prolonged elimination half life and good biocompatibility, and can be used as long-effect injection preparations for animals.
US20080166395 Pouches for nicotine replacement therapy; coconuts, flavors, herbs The present invention is an oral dissolvable pouch with a substrate, for providing therapy and a method of providing therapy using the pouch of the present invention.
WO2013139809A1 Use of a pyrazole derivative in the treatment of acute exacerbations of chronic obstructive pulmonary disease Use of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of acute exacerbations of chronic obstructive pulmonary disease. Treatment may involve a single dose of the active ingredient by oral administration.
CN101744834A Compound fructose electrolyte injection and preparation method and application thereof The invention provides a compound fructose electrolyte injection, which consists of the following raw materials in proportion by weight: 0.85 to 4.5 grams of anhydrous fructose, 0.35 to 0.65 gram of sodium chloride, 0.022 to 0.035 gram of potassium chloride, 0.02 to 0.025 gram of magnesium chloride, 0.42 to 0.7 gram of sodium gluconate, 0.25 to 0.5 gram of sodium acetate, and the balance of water for injection based on the total amount of 100 mL. The invention also provides a preparation method for the compound fructose electrolyte injection and application thereof. The compound fructose electrolyte injection is independent of insulin metabolism, and is very suitable to be used by diabetics and hepatopaths; the sodium acetate is used for replacing sodium lactate to avoid a large amount of lacticemia symptoms caused in the process of transfusion; the metabolism is stable so that the compound fructose electrolyte injection is suitable for wound and operation patients; besides, the compound fructose electrolyte injection has high energy and good safety.
WO2011023796A1 Bifeprunox for treating addiction The present invention relates to bifeprunox for use in the treatment of a patient with a substance use disorder, in particular wherein the substance is alcohol or nicotine and or food addiction, particularly where the addictive food is sucrose, a mono-or a polysaccharide.
CN102091324A Calcium for nourishing bones The invention discloses calcium for nourishing bones. The calcium provided by the invention is characterized by comprising the following components in parts by weight: 20-40 parts of enzymolyzed bone powder, 10-25 parts of xylose, 15-30 parts of bovine colostrum, 10-20 parts of pearl powder, 3-5 parts of collagen, 3-10 parts of magnesium stearate, 0.5-0.8 part of vitamin C, 1-5 parts of ammonia sugar and a trace amount of vitamin D and vitamin K. In the formulation provided by the invention, the calcium in a complexation state can be mostly absorbed by human bodies and utilized effectively, then the calcium in a molecular state can be absorbed by human bodies and utilized successively, and simultaneously the ammonia sugar is added, thus the immunocompetence of human joints can be strengthened obviously, the damage to joint organs caused by inflammatory factors can be impeded effectively, the substance metabolic balance in the joint organs can be maintained effectively, substances in a gristle synovial membrane are ensured not to bleed excessively, and the whole process of joint recovery can be completed radically. The calcium for nourishing bones is especially suitable for children and adults.
US20090069359 A formulation for treatment of alopecia contains minoxidil, urea, hydrocortisone and a skin desquamation agent comprising tretinoin Various medical conditions, some previously treated by injection or surgery, are effectively treated by a topical application of a composition of urea and a chemotherapeutic agent. Such agents include sclerosing agents, vasodilators, botulinum toxin and minoxidil. Conditions as diverse as spider veins, erectile dysfunction, facial wrinkles, hair loss and baldness can be effectively treated with the compositions.
CN1714874A Absorptive bone hemostatic agent The present invention discloses a kind absorptive bone hemostatic for surgical and orthopedic operation. The absorptive bone hemostatic includes mainly chitosan or modified chitosan 20-95 weight portions, konjaku glucomannan or carboxymethyl modified konjaku glucomannan 5-80 weight portions, and water in 50-500 % of total solid matter. It is prepared through mixing powder or water solution of the material. The absorptive bone hemostatic has simple operation, good compatibility, no irritation and inflammation reaction, and can induce bone growth.
WO2009145067A1 Therapeutic agent for pain and use thereof Disclosed are a therapeutic agent and a method for the treatment of pain, each of which utilizes a polynucleotide comprising a specific nucleotide sequence or a double-stranded polynucleotide containing the aforementioned polynucleotide as a functional polynucleotide. It becomes possible to achieve a technique for preventing pain.
US7166637 Hydroxyindoles, their use as inhibitors of phosphodiesterase 4, and processes for preparing them The invention relates to substituted 4- or/and 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active compounds for treating diseases which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 4 activity in immunocompetent cells (e.g. macrophages and lymphocytes).
WO2010066159A1 A preparation method of venlafaxine sustained release formulation A preparation method of venlafaxine sustained-release formulation is disclosed. It comprises the steps of dispersing venlafaxine and binder into isopropanol to form a suspension, spraying the suspension onto the sugar spheres to form the drug pellets, making aqueous suspension of talc and well mixing it with a polyacrylic resin water-dispersion, and then, spraying the talc-polyacrylic resin suspension onto the drug pellets to form said micropellet formulation with a slow-release coating.
WO2010039545A3 1,2-benzisothiazolinone and isoindolinone derivatives Novel classes of 1,2-benzisothiazolinone and isoindolinone compounds and compositions are disclosed. These compounds and compositions are useful in treating, preventing, and/or ameliorating viral, yeast, and fungal infections such as, for example, Hepatitis C Virus, Flavivirus infections, Aspergillus fumigatus, and candidiasis.
CN103626800A Fostrecin (FST) derivative and medical application and preparation method thereof The invention relates to a novel Fostrecin (FST) derivative represented by a general formula (I) shown in a drawing, medical application thereof and a preparation method thereof, and further relates to application thereof in preparation of pharmaceutical compositions for resisting tumor, inhibiting excessive cell growth or lowering myocardial infarction and injury to cells caused by myocardial infarction.
US20110184051 Pharmacological applications of mitochondrial dna assays The invention provides assays to determine the relative amount of mitochondrial DNA in a subject, such as a subject undergoing drug treatment. The subject may for example be a human patient undergoing treatment for an HIV infection with a nucleic acid precursor such as a nucleoside or nucleotide analogue. The assays of the invention may include PCR assays, such semi-quantitative or quantitative PCR involving the co-amplification of a mitochondrial sequence and a reference sequence, such as a genomic sequence. Information from such assays may be evaluated to provide a ratio of mitochondrial DNA to nuclear DNA in the cells of the subject.
CN103356621A Novel capsule filled with alogliptin solid preparation and pioglitazone solid preparation The invention relates to an oral-taking hard capsule, and in particular relates to a tablet capsule filled with an alogliptin tablet and a pioglitazone tablet. The tablet capsule comprises a capsule and tablets in the capsule, wherein the capsule contains an upper capsule body and a lower capsule body; at least one tablet taking alogliptin as an active component and at least one tablet taking pioglitazone as an active component are filled in the capsule. As the active components in the capsule are not in contact with each other, chemical compatibility among various components does not occur and a byproduct is not produced, so that the stability of the product is improved, especially a degradation product produced through the contact of alogliptin and pioglitazone is reduced, and related substances of the tablet capsule conform to the safety range of a human body.
EP2730572A1 Spiro compounds as hepatitis c virus inhibitors Disclosed are spiro compounds of formula (I), or stereomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof. The compounds can be used to treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore disclosed are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions in the treatment of HCV infection or hepatitis C disease.
CN103417809A TCM preparation for treatment of thrush in infants and children The invention discloses TCM preparation for the treatment of thrush in infants and children. Doctors of TCM reckon that thrush in infants and children is caused generally by brimming heat and deficiency fire and that the proper drugs for the treatment are effective in clearing heat-fire and nourishing yin to lessen fire. Therefore, the TCM preparation is made with meadowrue root and rhizome, common Souliea rhizome, tangut barberry bark, gypsum, common anemarrhena rhizome, herb of decumbent bugle, red peony root, and licorice root. Decoction of the TCM preparation is prepared in the preparation room of Yinan people's hospital; clinical experiments show that total effective rate is up to 100% and that the preparation has curative effect significantly better than that of a control group.
WO2014004676A1 Use of faah inhibitors as neuroprotective agents in the cns The present disclosure relates to methods of using a fatty acid amide hydrolase (FAAH) inhibitor of Formula I alone or in combination with one or more additional therapeutic agents for the treatment or prevention of neuronal injury or neurodegeneration in a patient in need thereof.
US20100190800 Combinaton of pyrimidylaminobenzamide compounds and imatinib for treating or preventing proliferative diseases The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) imatinib. and a method for treating or preventing a proliferative disease, especially GIST, using such a combination.
US7825247 an N-phenyl-4-(4-methyl-piperazin-1-ylmethyl)-benzamide claimed intermediate easily prepared by amidation of the aniline and the benzoic acid; reaction with a 2-aminopyrimidine to produce antitumor tyrosine kinase inhibitor The present invention relates to novel amides and a process for preparing these amides.
CN101926797A New application of tetrahydropalmatine derivatives The invention discloses new application of methyl-substituted tetrahydropalmatine derivatives. The new application is the application of the tetrahydropalmatine derivatives shown as a formula II or pharmaceutically-acceptable salts thereof to the preparation of medicaments for inhibiting eukaryotic tumor cell proliferation and the application to the preparation of medicaments for preventing and/or treating tumors. In-vivo anticancer activity test results indicate that the tetrahydropalmatine derivatives have the inhibiting effect on non-small cell lung cancer A-549 and small cell lung cancer H446 of humans, and the tumor volume of an administration group is smaller than that of negative control obviously. The results indicate that the tetrahydropalmatine derivatives shown as the formula II can be used for preparing medicaments for treating lung tumors, so that the medicinal application of the tetrahydropalmatine derivatives is widened.
EP0924986B1 Antioxidant derived from lentil and its preparation and uses Methods of obtaining and using an extract of lentil seed coats that are enriched in polyphenolic species are presented. The extract exhibits antioxidant activities against free radicals, including superoxide. The extract can be used to stabilize and protect food, animal feeds and dietary supplements against oxidizing agents. The extract can decrease the risk of conditions associated with free radical and oxidant stress and can limit the activity of proinflammatory cells.
WO2008059372A3 Crystal form of (3r,5r)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-metyl-benzylcarbamoyl)-2h-pyrazol-3-yl]-3,5-dihydroxy-heptanoic acid sodium salt A crystal form A of sodium; (3R, 5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl- benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dιhydroxy-heptanoic acid is provided.
WO2011079407A1 New compounds having potency to inhibit blood clotting Compounds of the following formula (1) or salts or stereoisomers thereof and method of preparation thereof, wherein, definition of R1, R2 and R3 are as described in description, and a pharmaceutical composition containing at least one of the compounds of formula (1) or salts or stereoisomers thereof as an active component are provided. The compounds have a potency to inhibit aggregation of the blood platelet, and can be used to prevent and treat thrombus and diseases related to embolism.
CA2181164C Anti-gram-positive bacterial methods and materials The present invention relates to methods of treating gram-positive bacterial infections by administration of a BPI protein product alone, or in combination with an antibiotic. BPI protein product alone has a bactericidal or growth inhibitory effect on selected gram-positive organisms. BPI protein product also increases the susceptibility of gram-positive organisms to antibiotics and can even reverse resistance of gram-positive organisms to antibiotic.
US20070259061 Extract oily phase by cold press and solvent; use as nutritional supplements, in cosmetics Subject of the invention is a process of manufacturing a selenium containing composition from selenium containing plant seeds comprising the step of extracting seeds of selenium containing plants with an apolar organic solvent yielding an extract wherein the selenium containing plants are selected from the group consisting of Lecythis ollaria Loeffling, Lecythis minor Jacquin, Lecythis usitata Miers, and Lecythis tuyrana Pittier, collecting the extract and substantially removing the apolar organic solvent yielding an oily phase having an insoluble residue, isolating the oily phase and the insoluble residue. Subject to the invention are further a method of cold pressing selenium containing plant seeds, selenium containing compositions and nutritional supplements.
US20070135354 Hematopoietic stimulation Methods and products for stimulating hematopoietic, preventing low levels of hematopoietic cells and producing increased numbers of hematopoietic and, mature blood cells are provided. The methods and products can be used both in vivo and in vitro.
CN102113997B Domperidone suspension and preparation method thereof The invention discloses a domperidone suspension, and each 1000ml of the suspension comprises the following components: 1g of domperidone, 6g-8g of sodium carboxymethyl cellulose, 8g-12g of microcrystalline cellulose, 0.3ml-0.7ml of polysorbate, 80g-120g of sorbierite, 1.5g-2.0g of methylparaben, 0.1g-0.3g of propylparaben, 0.1g-0.4g of saccharine sodium salt and the balance of water. The suspension is good in stability and redispersibility, has sweet flavor, can be preserved for 5 years, and is free of agglomeration.
CN101129412A Medicament for treating diarrhea of pigs The invention discloses a medicament for treating pig diarrhea, wherein the constituents include toxin expelling essence 10-15ml, Golden Thumb 10-12ml, VB 1-2ml, lactochrome sodium phosphate 1. 5-2mg, VB6 1. 5-2mg, niacinamide 25-30ml, dextro-calcium pantothenate 0. 5-1ml, racanisodamine hydrochloride injection 8-10mg.
US20080090889 Substituted 2-aminoalkylthiobenzimidazole compounds, pharmaceutical compositions thereof and methods for their use The present invention comprises the substituted 2-aminoalkylthiobenzimidazoles of formula I wherein R1-R5 and R11-R16 are hereinafter defined. These compounds, their derivatives and the pharmaceutically acceptable salts thereof are useful in the reduction of elevated blood sugar levels and are therefore useful in the treatment of hyperglycemia, diabetes, atherosclerosis and other blood sugar disorders. These compounds are particularly suitable in the treatment of type-2 diabetes.
CN101230068B Application of polyether triterpene compound in preparing medicine for treating tumour The invention relates to a polyether triterpene compound and the preparation method and the application thereof, and belongs to the antineoplastic medicine field. The specific structural formula is as shown in (I). The preparation method adopts the steps that marine red algae and laurencia decumbens kuetz are flushed, dried in shade, and crushed, and then extracted for 2 to 5 times by using an organic solution, the extracting solution is combined for concentration to obtain a crude extract; the crude extract is added into distilled water so that the crude extract is suspended in water, extraction with ethyl acetate is performed for 2 to 5 times, the extract is concentrated to obtain a corresponding extract, silicagel column chromatography is performed to the extract, the organic solution is used for elution, the eluent is collected and is detected through thinlayer chromatography; components eluted with 1-4: 1 gradient are separated and purified through silicagel column chromatographyto obtain a target compound I. The natural polyether triterpene compound obtained through extraction and separation by using the marine red algae and the laurencia decumbens kuetz belongs to a micromolecule natural organic compound, and is easy to be prepared and obtained, experiments show that the compound has remarkable antineoplastic activity, and can be used as antineoplastic medicine.
WO2013097773A1 Novel arylalkene derivatives and use thereof as selective estrogen receptor modulators The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.
CN1871239A Modulation of beta-catenin/tcf-activated transcription The present invention provides compounds and methods for modulating transcription activated by beta-catenin/TCF, such as the selective inhibition of genes targeted by the Wnt/beta-catenin pathway.
CN103483258A Geldanamycin analogue and application of same in preparing medicine for resisting tumor invasion and metastasis The invention provides a geldanamycin analogue and an application of the geldanamycin analogue in preparing a medicine for resisting tumor invasion and metastasis. The geldanamycin analogue is 17-demethoxy lebustatin, the molecular weight is 518.64, and the molecular formula is C28H42O7. The invention also provides an application of the 17-demethoxy lebustatin in preparing a clinical anti-tumor medicine. The 17-demethoxy lebustatin can be prepared into the preparation forms of intestinal or parenteral combined medicines according to the known method in the field of the preparation, the preparation forms mainly include a liquid preparation, a granule preparation, a tablet preparation, a dissolved medicine preparation, a gelatin pearl preparation, a capsule preparation, a sustained-release preparation, a dripping pill preparation or an orally disintegrating preparation, and the administration forms of the preparation mainly include oral administration or injection administration. The 17-demethoxy lebustatin provided by the invention is low toxicity, acts on the target point of Hsp90, can be used for effectively controlling the development and metastasis of the tumor, and is very good in application prospect of clinical anti-tumor medicines.
US20100255080 Liposomal ALA pharmaceutical and cosmeceutical compositions and methods of treatment Liposomal ALA pharmaceutical and cosmeceutical compositions, and methods of treatment are disclosed herein. In an embodiment, a Liposomal ALA composition of the present disclosure is used in for photodynamic therapy. In an embodiment, a photodynamic therapy system is disclosed that includes nanocorpuscles comprising 5-aminolevulinic acid in a scattering agent, wherein a concentration of the 5-aminolevulinic acid is from about 0.01% to about 10%; and a light source for activating the 5-aminolevulinic acid. In an embodiment, a photodynamic therapy method is disclosed that includes administering nanocorpuscles comprising 5-aminolevulinic acid to a target tissue in a patient; and activating the 5-aminolevulinic acid with a light source. In an embodiment, a kit is disclosed.
WO2009082819A8 Novel lupane derivatives The invention relates to 21-keto triterpene compounds of formula (I): wherein R1, X, and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
CN103623293A Micro-ecological oral preparation A disclosed micro-ecological oral preparation is composed of the following components in percent by weight: 5%-10% of lactobacillus acidophilus, 3%-7% of lactobacillus bifidus, 2%-7% of animal bifidobacterium, 12%-60% of galactooligosaccharide, 1%-28% of haw, 1%-28% of poria cocos, 1%-30% of fried malt and 1%-5% of honey powder. Lactobacillus acidophilus, lactobacillus bifidus and animal bifidobacterium are all powder with live bacteria number of 1010 cfu/g or more. Galactooligosaccharide comprises galactose and glucose which are generated by taking lactose in cow's milk as a raw material and performing catalytic hydrolysis on galactopyranoside by beta-galactosidase. The oral preparation aims at children with disordered gastrointestinal function and patients with disordered gastrointestinal function caused by long-term oral antibiotics, and is capable of rapidly enabling flora in intestinal tract to recover normal balance, adjusting micro-ecological balance of human body and improving health state of human body.
CN101397297A Aminothiazole derivates, preparation method and use thereof The invention relates to compounds with the structure of formula (I) or the acceptable salt of the compounds in pharmacy and a preparation method thereof. The invention also relates to the application of the compounds as medicines, especially as the anti-virus and anti-bacterial medicines. The invention further relates to aminothiazole derivatives and the preparation method and the application; wherein, the definition of each group is shown in the description in the instruction.
US20100056592 Prodrugs of (3,5-bis(4-fluorophenyl)tetrahydro-1h-oxazolo[3,4-c]oxazol-7a-yl)methanol and derivatives thereof A prodrug that has a prodrug moiety that degrades into a compound having the general Formula I with R3 being an alcoholic moiety can be useful in therapies for neurodegenerative diseases as well as cancer. Accordingly, the prodrug compounds can have a structure of Formula I, analogs thereof, derivatives thereof, or salts thereof, wherein: A and B are sulfur or oxygen; R1 and R2, in para, meta, or ortho position, are independently halogen, alkyl, alkoxy, haloalkyl, where R1 and R2 independently are straight chain, branched, substituted or unsubstituted; and R3 is a prodrug moiety. As examples, the prodrug can have a structure of any of Formulas I-V, which as shown in the specification.
US20060020046 Compositions comprising lycopene for the treatment and prevention of angiogenesis associated pathologies The invention is concerned with the use of lycopene, optionally in combination with vitamin E and/or C or other biologically active ingredients as disclosed in the specification, in the manufacture of a composition for the primary and secondary prevention of angiogenesis-associated pathologies and coadjuvant treatment thereof; as well as with particular novel formulations comprising lycopene.
CN1844130A Maple extract and its use in preparation of free radical scavenger or antioxidant This invention is about maple extracts' use in preparation of free radical scavenging agent and antioxidant. Its characteristic is as followings: in maple extracts, 2,6-2-gallic maple sugar ester is 20-95% in content; Gallicin 1-5%; isodulcitol flavonoid glycoside 1-10% and a little bit of carotenoid, sugar and chlorophyll. Maple extract is more efficient than other free radical scavenging agents and antioxidants. Its ID50 towards the free radical DPPH is no more than 1.0mg/ml. It could be used in various fields as food additives, commodity additives, oxidation resistance, antiaging agent, antiaging agent, sterilization, sulphanilamide and so on. This invention also provides a direction for new drug researches.
US20070298107 Pharmaceutical Compositions of Mirtazapine The present invention relates to pharmaceutical compositions of mirtazapine or its pharmaceutically acceptable salts. More particularly, the present invention relates to solid unit dosage forms of anhydrous mirtazapine or its pharmaceutically acceptable salts suitable for oral administration. The present invention also relates to a process for the preparation of pharmaceutical compositions of mirtazapine or its pharmaceutically acceptable salts.
EP2341058A2 Oligonucleotide Analogues The present invention relates to novel bicyclic and tricyclic nucleoside and nucleotide analogues as well as to oligonucleotides comprising such elements. The nucleotide analogues, LNAs (Locked Nucleoside Analogues), are able to provide valuable improvements to oligonucleotides with respect to affinity and specificity towards complementary RNA and DNA oligomers. The novel type of LNA modified oligonucleotides, as well as the LNAs as such, are useful in a wide range of diagnostic applications as well as therapeutic applications. Among these can be mentioned antisense applications, PCR applications, strand displacement oligomers, as substrates for nucleic acid polymerases, as nucleotide based drugs, etc. The present invention also relates to such applications.
CN1615847A Use of scopoletin in preparing medicine for preventing and curing hyperuricemia The present invention is application of scopoletin in preparing medicine for preventing and treating hyperuricemia causing gout, Lesch-Nyhan syndrome, hyperuricemia nephropathy, urinary calculus, cardiac vascular diseases, hyperlipemia and diabetes. It has obvious curative effect in administration via either injection or oral taking. It has no influence on normal serum uric acid, may be used as medicine for preventing hyperuricemia, can promote excretion of uric acid without diuresis effect, and has high treating effect on arthrocele and arthralgia caused by gout.
WO2012006551A3 Neuroprotective molecules and methods of treating neurological disorders and inducing stress granules Provided herein are neuroprotective molecules containing a sequence of 25-35 contiguous nucleotides that is at least 80% identical to a contiguous sequence between nucleotide 1 and nucleotide 50 of a mature human tRNA and at least four contiguous guanosine-containing nucleotides, where the sequence of 25-35 contiguous nucleotides contains a D-loop stem structure, the at least four contiguous guanosine-containing nucleotides are located at the 5' end of the neuroprotective molecule, and the neuroprotective molecule contains at least one deoxyribonucleotide. Also provided are molecules containing a sequence of 25-35 contiguous nucleotides that is at least 80% identical to a contiguous sequence between nucleotide 1 and nucleotide 50 of a mature human tRNA selected from the group of tRAArg, tRNAAsp, tRNAGln, tRNAGlu, tRNAGly, tRNAHis, tRNAIle, tRNALeu, tRNALys, tRNAMet, tRNAPro, tRNASeC, tRNASer, tRNASup, tRNAThr, tRNATrp, tRNATyr, tRNAVal, tRNAAsn, and tRNAPhe; and at least four contiguous guanosine-containing nucleotides, where the sequence of 25-35 contiguous nucleotides contains a D-loop stem structure and the at least four contiguous guanosine-containing nucleotides are located at the 5' end of the neuroprotective molecule. Also provided are methods of inducing or increasing stress granule formation in a cell, decreasing protein translation in a cell, decrease stress-induced cell death, or treating a neurological disorder associated with neuron death in a subject using at least one of these neuroprotective molecules or a C-myc oligonucleotide. Also provided are methods of identifying a candidate translation inhibitory nucleic acid.
US7189692 Synthetic peptides and pseudopeptides having osteogenic activity and pharmaceutical compositions containing the same Cyclic to Synthetic pseudopeptide derivatives of osteogenic growth polypeptide (OGP) and OGP(10-14) which are capable of enhancing bone cell proliferation and bone formation. Pharmaceutical composition comprising as active ingredient at least one pseudopeptide derivative of the invention and to the use of these pseudopeptide derivatives in the preparation of a pharmaceutical composition for stimulating the formation of osteoblastic or fibroblastic cells, enhancing bone formation in osteopenic pathological conditions, repairing fractures, healing wounds, grafting of intraosseous implants, reversing bone loss in osteoporosis and other conditions requiring enhanced bone cells formation.
CN103211786A Choline fenofibrate film-controlled enteric slow-release pellet capsule The invention relates to a choline fenofibrate film-controlled enteric slow-release pellet capsule. A slow-release film of the choline fenofibrate film-controlled enteric slow-release pellet utilizes Eurdragit RS 30D as a film-formation material. A pellet core of the choline fenofibrate film-controlled enteric slow-release pellet contains low-substituted hydroxypropyl cellulose having high expansibility, and also contains a pharmaceutically acceptable common excipient for the slow-release pellet, wherein preferably, the excipient comprises microcrystalline cellulose, and the pellet core comprises 10 to 40wt% of the low-substituted hydroxypropyl cellulose. The slow-release film comprises Eurdragit RS 30D, triethyl citrate as a plasticizer and talcum powder as an antiplastering aid, wherein preferably, a ratio of urdragit RS 30D to triethyl citrate to talcum powder is 30: 3: 4 and a film weight increasing ratio is in a range of 20 to 38%. The choline fenofibrate film-controlled enteric slow-release pellet comprises the pellet core containing low-substituted hydroxypropyl cellulose having high water expansibility and thus after absorbing water, the choline fenofibrate film-controlled enteric slow-release pellet expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the choline fenofibrate film-controlled enteric slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.
EP1712553A2 Derivates of [6, 7-dihydro - 5H - imidazo[1,2- alpha]imidazole-3-sulfonylamino]-propionamide and their use as inhibitors upon the interaction of CAMS and leukointegrins Derivatives of [6,7-dihydro-5H-imidazo[1,2α]imidazole-3-sulfonylamino]-propionamide of the formula I which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
CA2425779C Compositions that inhibit proliferation of cancer cells Disclosed are compositions and methods for reducing the proliferation of cancer cells through targeted interactions with integrins.
EP2132175B1 Process for the preparation of loperamide The current application discloses a process for the preparation of loperamide characterised in that glycerol formal is employed as a solvent.
US20110207757 Tricyclic Compounds Having Cytostatic and/or Cytoxic Activity and Methods of Use Thereof The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
US20060084612 Combined therapy against tumors comprising substituted acryloyl distamycin derivatives and protein kinase (serine/threonine kinase) inhibitors The present invention provides the combined use of acryloyl distamycin derivatives, in particular α-bromo- and α-chloro-acryloyl distamycin derivatives of formula (I), as set forth in the specification, and a protein kinase (serine/threonine and tyrosine kinases) inhibitor, in the treatment of tumors. Also provided is the use of the said combinations in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.
WO2011103202A3 Androgen receptor modulators and uses thereof Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors.
CN1830998A Total extractives of steroid saponin, prepn. method and application thereof The invention relates to extract of the steroid saponin produced from the yam or the yam with the guilder leaf which has the character of containing the 80%-90% the steroid saponin in the percentage by weight. The intravenous fluid produced from the extract of the steroid saponin can not only dilate the coronary, depress the myocardial oxygen consumption, melt the thrombus, improve the myocardial ischemia and the microcirculation, amend the function of the vas endothelial cell, increase the blood stream of the brain, prevent the ischemia brain cell injury, but also drop the blood pressure, the blood fat, the blood sugar; at the same time, it has the function of resisting inflammation, ease pain, codein, preventing asthma, dispelling the myospasm, improving the immunity and resisting the allergy. So it can cure the cerebrovascular, the rheumatism and the disease of the respiratory system. The invention has the good clinic extended value because of the low dosage of the active ingredient, the efficacy, the effecting quick and the high bioavailability.
CN1823782A Long effect oxyfluoroshaxin nano-capsule injection liquid for animal and its preparation method A long-acting nanosac-type injection of ofloxacin as veterinary medicine is prepared through mixing ofloxacin with the aqueous solution of arabic gum, stirring, adding the aqueous solution of acetic acid while stirring to generate the coagulative sac solution, adding the water for injection, cooling, adding the aqueous solution of formaldehyde to become solidified sacs, water washing and adding the water for injection.
WO2010106028A1 Use of a kinase inhibitor for the treatment of thymoma The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents.
CN103202826A Benzalkonium chloride and sodium bicarbonate composite disinfectant The invention discloses a benzalkonium chloride and sodium bicarbonate composite disinfectant. The benzalkonium chloride disinfectant is prepared from benzalkonium chloride, sodium bicarbonate and water for injection. The disinfectant comprises the following components in percentage by weight: 0.23-1.0% of benzalkonium chloride, 0.01-1% of sodium bicarbonate and the balance of water for injection. The disinfectant is specially used for disinfecting skins before operation, cleaning and disinfecting mucous membranes and wounds, treating trauma and burn injection, and disinfecting and storing operative apparatuses. According to the disinfectant, serolemma permeability is changed, so that spore materials are leaked to prevent metabolism to kill. The disinfectant has stronger effect to gram positive bacteria, Pseudomonas aeruginosa, acid-fast bacillus and bacterial spore, and not only meets the disinfecting concentration of benzalkonium chloride disinfectant at 0.23-1%, but also does not strongly irritate skins to reduce paint of the patient, so that contradiction of high concentration with disinfecting effect and skin irritation is solved.
EP1319008B1 Water soluble rapamycin esters This invention provide pegylated hydroxyesters of rapamycin which are useful in inducing immunosuppression and in the treatment of transplantation rejection, autoimmune diseases, solid tumors, fungal infections, and vascular disease.
US20080214480 Method for Treating Sickle Cell Disease and Sickle Cell Disease Sequalae The present invention is directed to methods of treating sickle cell disease and its sequelae, including vaso-occlusive crisis. The method comprises administering to a subject in need thereof a pharmaceutical composition comprising an elective amount of a polyanionic polysaccharide, such as pentosan sulfate, sulodexide, or its pharmaceutically acceptable salts thereof. The methods of the present invention are useful in reducing the incidence, severity, or duration of SCD and its sequelae. The compound of the present method can also be used in conjunction with other therapeutic agents useful to treat sickle cell disease thus enhancing the therapeutic elect of reducing the required dosed to treat sickle cell disease.
US20080194551 Acetylene Derivatives The invention provides compounds of formula (I), wherein the substituents are as defined in the specification, to processes for their preparation and their use as pharmaceuticals.
US7592305 Use of ghrelin for treating malnutrition in gastrectomized individuals The present invention relates to use of ghrelin or an analogue thereof for the preparation of a medicament for one or more of: treatment and/or prevention of loss of body weight and body fat, prophylaxis or treatment of cachexia, stimulation of appetite, stimulation of food intake, stimulation of weight gain, or increasing body fat mass, in a gastrectomized individual.
WO2009026794A1 Cyclohex-enone compounds from antrodia camphorata for protecting liver The invention discloses acyclohex-enone compounds from antrodia camphorata, in particular 4-hydroxy-2,3-dimethoxy-6-methy-5[3,7,11-trimethyl-dodeca-2,6,10- trienyl]-cyclohex-2-enone, which can protect hepatic tissue effectively. In the invention, the acyclohex-enone compounds from antrodia camphorata for protecting liver have the effects of relieving the injure and fibrosis of liver induced by chemical liver injure, decreasing the concentration of ALT and AST, increasing the concentration of GSHPx and CAT, decreasing the injure of hepatic cell induced by free radical, improving the antioxidative effect of hepatic tissue.
CN102961348A Preparation method of gliclazide-containing medicament for treating diabetes mellitus The invention relates to the field of medicaments and particularly relates to a preparation method of a gliclazide-containing medicament for treating diabetes mellitus. The problem to be solved is to provide the preparation method of the gliclazide-containing medicament for treating diabetes mellitus. The adopted technical scheme is as follows: weighing raw materials in parts by weight: 9-10 parts of gliclazide, 15-25 parts of hydroxypropyl methylcellulose, 5-10 parts of milk sugar, 15-20 parts of calcium hydrophosphate and 0.5-1 parts of magnesium stearate; then mixing the materials, tabletting and preparing gliclazide tablets. The preparation method of the gliclazide-containing drug for treating diabetes mellitus is widely applied to the pharmaceutical field of the gliclazide.
CN102936233A New crystal form of 1-[di(4- fluorophenyl)methyl]-4-(2,3,4-trimethyl phenyl) piperazine dihydrochloride The invention provides a new crystal form of 1-[di(4- fluorophenyl)methyl]-4-(2,3,4-trimethyl phenyl) piperazine dihydrochloride. The melting point of the new crystal form ranges from 149 DEG C to 151 DEG C, the new crystal form is amorphous, and no obvious heat absorption peak is shown in a DSC (differential scanning calorimetry) diagram. The invention further provides a medical preparation containing the new crystal form and application of the medical preparation. The new crystal form has excellent biological utilization rate and efficacy, good in stability, not easy to transform on preservation condition, and is the excellent crystal form for preparation.
EP1751119A1 Novel fused heterocycles and uses thereof This invention relates to novel compounds having the Formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of H. pylori infection.
WO2009080223A1 Cyclic pyridyl-n-(1,3,4)-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals The invention relates to cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. What is described are compounds of the Formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
WO2012011592A1 Heterocyclic compound and application thereof Disclosed is a compound that has delta-5-desaturase-inhibiting activity, is useful in the prevention/treatment of conditions such as arteriosclerosis, diabetes, and obesity, and has excellent efficacy. The compound is the compound represented by formula I (in the formula, each symbol is as described in the specification) or a salt thereof.
US20110245243 Compounds and compositions as cathepsin s inhibitors The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.
CN102670573A Application of curcumin derivative in preparation of drug for treating prostate cancer disease The invention relates to application of a curcumin derivative Ca 37 in preparation of a drug for treating a prostate cancer disease, and relates to the field of biology and pharmacy. The object is to provide a use of the curcumin derivative in treatment of the prostate cancer disease. The application provided by the invention is mainly characterized in that the proliferation of prostate cancer cells PC(Prostate Cancer)-3 which are independent of male hormones is inhibited by the curcumin derivative, and the effect is obviously better than that of curcumin itself, the decrease of the capacity function of the PC-3 cells, i.e., oxygen glycolysis and oxidative phosphorylation, apoptosis starting and autophagy defects are induced, and the growth inhibition function mainly depends on the generation of reactive oxygen species.
CN103372178A Medicament and preparation method thereof The invention relates to the field of health products, and discloses a medicament. The medicament comprises main components of natural precious herbs such as morinda officinalis, herba cistanche, gastrodia elata, eucommia ulmoides, polygonum multiflorum, saffron crocus, medlar, angelica sinensis, rhizoma polygonati, pseudo-ginseng, lucid ganoderma, ginseng and the like. The invention also discloses the content of each component. The medicament comprises a plurality of effective ingredients of panaxoside, panaxadiol saponin and the like, has the functions of improving blood microcirculation, relieving and balancing cranial nerve, smoothing lymph to expel toxin, and promoting metabolism, contains starch, protein, fat, tannin, flavonoids compounds, phenolic compound and trace volatile oil, and also contains microelements iron, zinc and the like with biological activity; the leaf and stem contain a little of alkaloid, which has the functions of whitening the skin, resisting fatigue and caducity, improving mental sleep, physical power and function, and the like. The invention also discloses a preparation method of the medicament disclosed by the invention. The method comprises the steps of selecting materials, cleaning, fertilizing, drying and mechanically crushing. The process is advanced and unique; the dosage form can be changed; any other chemical reagent is not added; the medicament is environment-friendly.
EP1001760B1 Composition for controlling mood disorders in healthy individuals The use of acetyl L-carnitine and its pharmacologically acceptable salts is disclosed for producing a composition suitable for controlling mood disorders mainly in young individuals who are not affected by permanent pathological CNS disturbances.
US20100008866 Cis-cyclohexyl substituted pyrimidinone derivatives Cis-cyclohexyl substituted pyrimidinone derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
CN102552278A Medicinal composition for enhancing solubility of slightly-soluble medicament tolvaptan The invention relates to a medicinal composition for enhancing the solubility of slightly-soluble medicament tolvaptan. According to the medicinal composition, the solubility of tolvaptan can be enhanced effectively. Tolvaptan solid preparations such as tablets are prepared with a micronization technology and a pharmaceutically-acceptable diluent or carrier, and slightly-soluble tolvaptan is quickly released from the preparations, so that the bioavailability is improved. Compared with a disclosed preparation process for improving the solubility of tolvaptan, a process used in the invention has the advantages of easiness, practicability, no use of any organic solvent in a process, reduction in the cost, and reduction in environmental pollution.
WO2008104734A1 Treatment of anxiety disorders with minocycline The present invention relates to the use of a minocycline compound or a prodrug thereof; or a pharmaceutically acceptable salt thereof; in the manufacture of a medicament for the treatment of an anxiety disorder in children or adolescents.
CN103690535A Application of demethyleneberberine hydrochloride in preparation of medicament for preventing and/or treating hepatic fibrosis The invention discloses application of demethyleneberberine hydrochloride shown as a formula (I) in preparation of a medicament for preventing and/or treating hepatic fibrosis.
US20110038910 Anti-infective antimicrobial-containing biomaterials Fatty acid-derived biomaterials, methods of making the biomaterials, and methods of loading them with silver compounds are described. The silver-containing biomaterials can be utilized alone or in combination with a medical device for the release and local delivery of one or more anti-infective agents. Methods of forming and tailoring the properties of said biomaterials and methods of using said biomaterials for treating injury in a mammal are also provided.
CN102038684A Drug composition for relieving cough and reducing phlegm The invention relates to a drug combination for relieving cough and reducing phlegm, which is composed of active constituents and a pharmaceutic adjuvant, wherein the active constituents comprise butamirate critrate, dextromethorphan hydrobromide and guaifenesin. The composition can be prepared into various kinds of oral preparations such as granules, troches, capsules, oral solution, syrup and the like and can be used for carrying out symptomatic treatment on related diseases with symptoms of cough, abundance of phlegm and the like.
US20080107661 Using cell free system for identifying agents which prevent mucin and chronic myelogenous leukemia ligand binding; antitumor agents; treating cell proliferative, nervous system, inflammatory and atherosclerotic disorders The present disclosure provides methods of identifying and making compounds and pharmaceutical compositions thereof that inhibit the interaction between MUC1 and Abl. The invention also provides in vivo, in vitro, and ex vivo methods of inhibiting such an interaction. Also featured are in vitro and in vivo methods of stimulating the Abl-dependent apoptotic pathway in cells expressing MUC1. In such methods, the compounds, compositions, and methods described herein are generally useful in the treatment of various cancers. The disclosure also provides methods for inhibiting Abl, and such methods, and compounds and compositions for use in the methods are generally useful for the treatment of cancers, inflammatory conditions, atherosclerotic lesions, and neurologic disorders.
US20110097390 Ultra-Small RNAs as Toll-Like Receptor-3 Antagonists Provided are methods and compositions for the treatment or prevention of macular degeneration or other diseases or disorders associated with activation of TLR3. Administration of double stranded RNAs having a length of 22 nucleotides or less treats or prevents macular degeneration or other diseases or disorders associated with activation of TLR3 due to the ability of the RNAs to bind to but not activate TLR3. Furthermore, all double stranded RNAs (both targeted and non-targeted) of 22 nucleotides or less in length can bind to but not activate TLR3 and thereby treat or prevent such conditions. Also provided of a method for increasing the specificity of a desire siRNA target knockdown, the method comprising administering an amount of a target siRNA sufficient to knockdown a target gene and an amount of a double stranded RNA of 22 nucleotides or less which prevents the target siRNA from activating TLR3.
CN102125533A Pazufloxacin mesylate tablet and preparation method and detection method thereof The invention relates to a pazufloxacin mesylate tablet and a preparation method and a detection method thereof, which belong to the technical field of medicines. A medicinal oral tablet with high dissolvability and high stability is prepared by the following steps of: screening the formula components of the pazufloxacin mesylate tablet; and selecting suitable adhesives and adopting specific coating materials. Clinical trials show that the pazufloxacin mesylate tablet has an exact curative effect, a few side effects and high safety.
WO2005058323A1 USE OF METABOTROPIC GLUTAMATE RECEPTOR 1 (mGLuR1) ANTAGONISTS FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME (IBS) The present invention relates to the use of metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of irritable bowel syndrome (IBS).
CN103110639A Preparation method of capsule containing tegafur, gimeracil and potassium oxonate The invention relates to a preparation method of a capsule containing tegafur, gimeracil and potassium oxonate. The preparation method is characterized in that gimeracil is added in a form of micronized solid. The preparation method related by the invention overcomes bad water solubility of gimeracil by utilizing a micronized technology, thus the improvement of medicament dissolution is facilitated.
US20120295955 Rna antagonist compounds for the modulation of her3 The invention relates to oligomer compounds (oligomers), which target HER3 mRNA in a cell, leading to reduced expression of HER3 and/or HER2 and/or EGFR. Reduction of HER3 and/or HER2 and/or EGFR expression is beneficial for a range of medical disorders, such hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of HER3 and/or HER2 and/or EGFR using said oligomers, including methods of treatment.
EP2314585A1 Condensed benzamide compounds as inhibitors of vanilloid receptor subtype 1 (VR1) activity To provide a compound having an excellent inhibitory effect on vanilloid receptor subtype 1 (VR1) activity which is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, acute pain, chronic pain, neuropathic pain, rheumatoid arthritis pain, neuralgia, etc. and a pharmaceutical composition containing the compound. The object has been attained by a condensed benzamide compound represented by the following formula (the symbols in the formula have the same meanings defined in the specification) or its salt:
CN103393705A Application of scutellarin in preparing medicines for preventing and treating Alzheimer's disease The invention discloses an application of scutellarin in preparing medicines for preventing and treating Alzheimer's disease. Alzheimer's disease (Alzheimer's Disease, AD) is a neurodegenerative disease, the pathological features of which are that neurofibrillary tangles in the cells, and proliferation of reactive microglial cells and neurogliocytes are formed, wherein the principle reason of AD is deposition of extracellular amyloid protein Abeta. According to the invention, the level of Abeta in brain and serum of mice eating scutellarin-containing AD is remarkably reduced, and amyloid plaques and microglial cells in brain tissues are further remarkably reduced, so that scutellarin can prevent deposition of Abeta and weaken active components of inflammation of brains of mice with AD.
EP2673262A1 Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.
CN101036655A Stable cefoperazone potassium clavulanatein medicine compound preparation The invention discloses a stable compound preparation of cefoperazone-piperacillin clavulanate drug, which is comprised by cefoperazone acid, piperacillin clavulanate and latent solvent, which weight ratio is 16~1:1:8.8~0.06. The latent solvent is preferred selected from sodium carbonate and sodium bicarbonate. Related substances content of the compound preparation, labelled content of the cefoperazone acid and the piperacillin clavulanate in the invention do not change much in influencing factor test, long-term sample tests and accelerated test in 40 DEG C. which accord with the standard of pharmacopoeia with stable product quality.
US20110054020 Napthylene inhibitors of cyclooxygenase The present invention relates to new napthylene inhibitors of cyclooxygenase activity, pharmaceutical compositions thereof, and methods of use thereof
US20110263515 Capture agents and related compositions, methods and systems Multi-ligand capture agents comprising two or more ligands are described, and related compositions, methods and systems.
WO2014003677A1 Pharmaceutical compositions comprising solid dispersion particles containing tadalafil The present invention relates to pharmaceutical compositions comprising solid dispersion particles containing tadalafil and a dispersing component; which composition further optionally comprises a pharmaceutically acceptable solubilizer. Further, the present invention relates to a method of treating disorders in a patient in need thereof, comprising administering a therapeutically effective amount of said composition.
US20090214682 Composition and methods for weight loss in a subject The present invention relates generally to weight loss compositions and more particularly to orally administrable weight loss compositions for supporting weight loss in a subject in need thereof. Specifically, the present invention relates to compositions and methods comprising various combinations of orlistat and substances selected from methylxanthines, extracts of Morus sp., chromium polynicotinate, hydroxycitric acid or derivatives of hydroxycitric acid, flavanols, and yohimbine or derivatives of yohimbine.
WO2009093595A1 Method for producing carotenoid-containing emulsion composition, carotenoid-containing emulsion composition obtained by the same, carotenoid-containing powder composition, and functional food and cosmetic preparation each containing the composition Disclosed is a method for producing a carotenoid-containing emulsion composition, which comprises a step of performing emulsification and dispersion in an inert gas atmosphere by using a water phase, which is obtained by mixing an aqueous medium containing deoxidized water with a water-soluble emulsifier, and an oil phase containing carotenoid.
US20110306666 New plant derived seed extract rich in essentially fatty acids derived from salvia hispanica l. seed: composition of matter, manufacturing process and use A Salvia hispanica L. derived seed oil extract composition of matter containing from 60-88% PUFAs in a ratio of from 3.1:1-3.3:1 of ALA to LA, 4-10% of C-18 mono-unsaturated fatty acid, 1-5% of C-18 saturated fatty acid and 4-8% of C-16 saturated fatty acid in a mixed triglyceride form stable at room temperature of 12-24 months containing a mixture of selected antioxidants.
WO2014146486A1 Three-level cyclic amine alk kinase inhibitor for treating cancer Provided are substituted cyclic amine compounds, and pharmaceutically acceptable salts and pharmaceutical preparations thereof as an anaplastic lymphoma kinase (ALK) inhibitor. Also provided is the use of the compound and pharmaceutical preparations thereof in the preparation of drugs for the treatment and inhibition of diseases including non-small cell lung cancer (NSCLC), neuroblastomas, anaplastic large cell lymphoma (ALCL), liver cancer and other diseases caused by the rise of the ALK activity level.
EP1235899B1 Treatment of human infertility Human infertility can be treated by in vitro methods that actively arrest the human oocyte in prophase of first meiotic division and subsequent actively reversed this meiotic blockage by either adding at least one meiosis-stimulating compound or by culture conditions leading to endogenous formation of meiotic stimulating molecules in the oocyte-cumulus complex.
WO2007120595A3 Amines for the treatment of hcv The present application describes organic compounds (Formula (I)) that are useful for the treatment of human hepatitis C Virus (HCV).
US7078515 Sodium-channel alpha1-subunit and their polypeptides and their treatment of generalized epilepsy with febrile seizures plus The mutations D188V, V1353L, I1656M in the neuronal gene sodium-channel alpha1-subunit, SCN1A, are disclosed. The methods of using their associated polypeptides for treating sodium channel dysfunction disorders including generalized epilepsy are also disclosed.
WO2006087173A1 Contraceptive pharmaceutical preparation The invention relates to a pharmaceutical composition containing dienogest at an amount that corresponds to a daily dose unit of 1.5 mg or 2.0 mg when the composition is administered and ethinyl estradiol at an amount which corresponds to a daily dose unit of 0.015 mg or 0.020 mg when the composition is administered, together with one or several pharmaceutically acceptable carriers for at least 21 daily dose units. The invention further relates to an oral contraceptive pharmaceutical preparation containing 1.5 mg of 17α-cyanomethyl-17-ß-hydroxyestra-4,9-dien-3on (dienogest) and 0.015 or 0.020 mg of 17a-ethinyl estradiol (ethinyl estradiol) or 2.0 mg dienogest and 0.015 mg ethinyl estradiol along with one or several pharmaceutically acceptable carriers for at least 21 daily dose units of a 28-day menstruation cycle.
WO2006125778A1 Novel trifluoromethoxy-substituted aryl anilides The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or disorders associated therewith.
EP1497294A1 1,2,3,4,7,8-HEXAHYDRO-6 i H /i - 1,4 DIAZEPINO 6,7 ,1- i 1J /i QUINOLINE DERIVATIVES AS ANTIPSYCHOTIC AND ANTI OBESITY AGENTS Compounds of formula I or a pharmaceutically acceptable salt thereof are provided where R1 through R7 are defined herein. The compounds of formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
US20080207555 Catalyzing the release of ADP-ribose from poly(ADP-ribose) or O-acetyl-ADP-ribose by contacting with an isolated ARH3 polypeptide; modifying DNA repair or chromatin structure by modifying ARH3 polypeptide activity; drug screening; antiinflammatory, antiischemic agents; aging resistance This disclosure provides methods for catalyzing the release of ADP-ribose from poly(ADP-ribose) or O-acetyl-ADP-ribose. Also provided are methods for modifying DNA repair or chromatin structure by introducing into the cell an agent that modifies the activity of an ARH3 polypeptide, or variant or fragment thereof. Further provided are methods for screening molecules involved in the poly(ADP-ribosyl)ation of proteins or O-acetyl-ADP-ribose content, and method for treating disorders by altering activity of an ARH3 protein.
WO2014081689A1 Compounds useful as inhibitors of indoleamine 2,3-dioxygenase The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications.. The compounds of this invention have formula I-A; wherein the variables are as defined herein.
WO2009134725A3 Monomethylamine progesteron antagonists such as cdb-4453 in the treatment of endometriosis, uterine fibroids, dysmenorrhea, breast cancer etc The subject matter of the instant invention is pertinent to the field of treatment of progesterone-dependent conditions. Compositions for practicing the methods, comprising one or more 19-norsteroid progesterone receptor modulators having a monomethylamine-substituted phenyl ring at the 11 β-position of carbon 11 and exhibiting low antiglucocorticoid activity, are also disclosed. Embodiments of the instant invention disclose methods for treating endometriosis, dysmenorrhea, breast cancer, uterine fibroids and endometrial hyperproliferation.
US20100311784 Stereoselective process and crystalline forms of a camptothecin A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process.
US20070167424 Aztreonam L-lysine and methods for the preparation thereof The present invention relates to the L-lysine salt of aztreonam and methods for making the L-lysine salt of aztreonam.
US20050202101 Method and composition for preventing or reducing the symptoms of insulin resistance syndrome A method for preventing and or reducing the symptoms of insulin resistance and a related syndrome in persons comprises identifying persons having or at risk for having such symptoms, and administering to them an effective amount of a composition comprising chromium bound niacin that prevents or reduces the symptoms. Compositions incorporating chromium bound niacin and additional compounds also are disclosed that are particularly effective in preventing or reducing these symptoms.
US20100137431 Use of substances that act as cascade inhibitors of the raf/mek/erk signal cascade, for producing a medicament to treat dna and rna viruses The invention consists in that substances acting as cascade inhibitors of the Raf/MEK/ERK signaling pathway, in particular MEK inhibitors, are used for the production of a drug for the preventive and antiviral therapy against DNA and RNA viruses, in particular against intranuclear-replicating negative strand RNA viruses, for instance influenza or Borna disease viruses.
CN101869549A Oral sustained-release dry suspension taking roxithromycin as main ingredient The invention relates to oral sustained-release dry suspension taking roxithromycin as a main ingredient. The oral sustained-release dry suspension is prepared from the roxithromycin serving as the main active ingredient and pharmaceutically acceptable supplementary materials by pharmaceutical technology. The oral sustained-release dry suspension of the invention has the advantages of greatly increasing the patient compliance, reducing the number of missing taking medicine, along with stable and controllable quality, safety and effectiveness.
WO2006119390A1 Pyridines useful as modulators of ion channels The present invention relates to compounds of formulae I-A to I-D useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
US8314090 Methods of synthesis of benzazepine derivatives The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.
WO2006073202A9 METHOD OF TUMOR SUPPRESSION AND EVALUATION OF ANTICANCER AGENT BASED ON GSK3β INHIBITORY EFFECT It is intended to provide a novel means of treating and diagnosing cancer by clarifying the participation of glycogen synthase kinase 3β (GSK3β) in the survival and proliferation of cancer cells. Namely, a method of suppressing the survival and proliferation of cancer cells by inhibiting the expression of GSK3β or the activity of the above-described enzyme having been activated by the phosphorylation at the 216th tyrosine residue thereof; and a method of developing a novel anticancer agent and a method of evaluating an anticancer agent based on the inhibitory effect as described above.
CA2830616A1 Pharmaceutical composition for treating hepatic disease A pharmaceutical composition for alleviating aggravation of hepatoma, improving hepatic function, improving hepatic fibrosis, improving hepatic cirrhosis, improving hepatitis and promoting injured liver regeneration is provided by the present invention. The pharmaceutical composition comprises an effective amount of procyanidin and a pharmaceutically acceptable carrier or salt, wherein the chemical formula of the procyanidin monomer is as follows. In the chemical formula, when R1 is OCH3, R2 is OH, R3 is H, or when R1 is OH, R2 is H, R3 is H, or when R1 is OH, R2 is OH, R3 is H, or when R1 is OH, R2 is OH, R3 is OH, and R4 is 3-(alpha)-OH, 3-(beta)-OH, 3-(alpha)-O-sugar or 3-(beta)-O-sugar.
WO2013188786A1 Compositions and methods for treating airway inflammatory diseases A composition for treating an airway inflammatory disease having high molecular weight, crosslinked hyaluronan and optionally at least one aeroallergen is provided. A method of inducing immune tolerance to one or more aeroallergens in a mammalian subject suffering from or at risk of developing an airway inflammatory disease, and a method of treating a human subject suffering from or at risk of developing an airway inflammatory disease or condition of the lungs are also provided.
CN101380393B Ointment for treating pharyngitis and preparation method thereof The invention provides an ointment which treats pharyngitis and a preparation method thereof, more particularly relates to a drug which treats pharyngitis. The drug overcomes the defects in the treatment of pharyngitis with other drugs and is prepared from the following crude drugs of licorice, coptis, radix clematidis, blackberrykiky rhizome, musk and Chinese mugwort and the auxiliary materials of honey, balm, white sugar and a silverware. The preparation method comprises the following steps: licorice, radix clematidis, blackberrykiky rhizome, coptis and Chinese mugwort are put into a boileraccording to the requisite amount, and 10 kilos of water is added into the boiler, and firstly the boiler is boiled up with big fire and the decoction is carried out for 2 to 3 hours with small fire;then the decocted liquid medicine is filtered, and balm, white sugar, honey and a silver ring are added into the liquid medicine after the medical slag is removed, and the silver ring is knotted witha cord and is boiled into a dark brown solid with small fire and the silver ring is taken out when the medicine is to be boiled; packing: a glass bottle or a plastic bottle is used for packing with 1,500g/bottle; storage: sealing is carried out, and the medicine is put in shady places.
CN101244093A Method of preparing shiitake fungus polyoses oral liquid The invention relates to a preparation method of mushroom polysaccharide oral liquid which is characterized in the following steps: mushroom section, heating extraction, concentration, alcohol precipitation, high-speed centrifugation, concentration and getting small molecular weight mushroom polysaccharide oral liquid. The oral liquid is characterized in that the obtained mushroom polysaccharide oral liquid removes big molecular structure which is not suitable for absorption, not easy to produce gastrointestinal inflation, promoting gastrointestinal absorption, enhancing effect of the product and no side effect, convenient using, quality assurance.
WO2014090709A1 Dimeric compounds Disclosed are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein Z, X, Q and R1 are as described in this application, and methods of using the compounds in the treatment of cancer.
CN101830895A Aztreonam anhydrous crystal compound and preparation method thereof The invention provides an aztreonam anhydrous crystal compound. An X-ray diffractive map comprises the following X-ray diffractive peaks: 18.2 degrees +/- 0.2 degree, 24.0degrees +/- 0.2 degree, 9.1 degrees +/- 0.2 degree, 4.1 degrees +/- 0.2 degree and 17.2 degrees +/- 0.2 degree disclosed by 2 theta angles. The invention also provides a method for preparing the aztreonam anhydrous crystal compound. The aztreonam anhydrous crystal compound has a sharp outline, can be perfectly reappeared, has powder flowbility, intrinsic dissolution rate, solid stability, and the like which are obviously better than that of the traditional aztreonam crystal compound and can be prepared into a medical composition for treating various types of infection caused by sensitive oxybiontic gram-negative bacteria.
CN101264056A Epirubicin hydrochloride liposome and preparation thereof The invention belongs to the medicine technical field, relates to epirubicin hydrochloride liposome and a preparation method. The liposome comprises epirubicin hydrochloride and neutral phospholipid and cholesterol and/or negative charge phospholipids and/or long-circulating phospholipids and buffer solution, and actively carries drug with a PH gradient method or an ammonium sulphate gradient method; the entrapment rate of the achieved liposome is more than 90%, to make smaller volume contain more main drug component of epirubicin. Compared with the exiting techniques, the epirubicin hydrochloride liposome and the preparation method has the advantages of high drug content, high bioavailability, long internal circulation time, low toxic and side effect and other advantages; besides, the production cost can be reduced obviously, the epirubicin hydrochloride liposome is more suitable for industrial production after being made into lyophilized preparation. The liposome is clinically suitable for the tumor therapy, in particular to the tumor therapy for children.
CN102847090A Preparation process of integration-type novel formulation of Flos Inulae and hematite decoction and production method thereof The invention relates to a preparation process of integration-type novel formulation of Flos Inulae and hematite decoction and a production method thereof. The effective components of the novel formulation are made from the following raw materials (by weight parts): Flos Inulae (Inula britannica and/or Inula linariaefolia) 9, Radix Glycyrrhizae Preparata 6, Radix Codonopsis (Codonopsis pilosula and/or Codonopsis tangshen) 9, processed Pinellia ternate 9, Zingiber officinale 9, hematite 15, Ziziphus jujuba (Fructus Jujubae) 4. The production method includes the steps of supersonic airstream pulverization, alcohol-water extraction, ultrasonic pulverization and extraction, water decoction and concentration, supersonic spray-drying, nano-scale grinding, high-pressure emulsion and homogenization and nanoparticle preparation. The production method integrates the advantageous of the nano-carrier combination technique, such as multi-component synergism and multi-target. The large-scale production can greatly reduce the production cost, greatly improve the product quality and enhance the target property and sustained/controlled-release property of drugs. The novel formulation is administered by oral intake and external application during four time periods respectively based on the midnight-noon tidal flow and human qi-blood flow rule. The novel formulation is also processed to membranes and transdermal delivery agents which are applied to different parts of human body respectively according to the midnight-noon tidal flow and human qi-blood flow rule and can be directly absorbed by the skin.
US20110206734 Hybrid scfa-hydroxyl-derivatized monosaccharides, methods of synthesis, and methods of treating disorders Described herein are fatty acid carbohydrate-hydroxyl-hybrid compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof.
WO2012000212A1 Compound for inhibiting type 5 phosphodiesterase and preparation method thereof A compound of formula (I) and citrate thereof as inhibitors of type 5 phosphodiesterase (PDE5), their preparation methods, and a pharmaceutical composition comprising the compound of formula (I) and citrate thereof are disclosed in the present invention. The trial of the present invention proves that the compound of formula (I) and citrate thereof can inhibit the activity of PDE5 and can be used for treating erectile dysfunction, inhibiting platelet aggregation and treating thrombosis, decreasing pulmonary artery hypertension and treating cardiovascular diseases, treating asthma and treating diabetic gastroparesis.
CN102727487A Novel application of 8-methoxsalen to prevention and treatment of osteoporosis for post-menopause women The present invention relates to novel application of 8-methoxsalen to the pharmaceutical field, and particularly to preparation of medicine for preventing and treating osteoporosis. The invention includes an oral preparation, prepared from combination of 8-methoxsalen and clinically applicative calcium preparation or phosphonate, for clinical treatment of osteoporosis, and also includes a tablet, a capsule, a granule, an oral liquid, an injection, intravenous and intramuscular injection preparations, a liposome preparation and a microcapsule, prepared from combination of 8-methoxsalen and clinically acceptable drug carrier, for treatment of osteoporosis.
WO2014078408A1 Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
WO2008001182A8 Tricyclic heteroaryl compounds as pde10 inhibitors The invention pertains to tricyclic heteroaryl compounds of formula (I) that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds which are selective inhibitors of PDElO. The invention further relates to pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom.
WO2011030847A1 Inducer composition for hematopoietic stem cells Provided is an inducer composition for hematopoietic stem cells, which contains a thiazolidine compound or salts thereof having nuclear receptor PPARγ agonist activity, and which serves to increase the number of hematopoietic stem cells in a subject. The inducer composition for hematopoietic stem cells can increase the number of hematopoietic stem cells for bone-marrow transplantation, and also increase the number of peripheral blood hematopoietic stem cells in combination with a hematopoietic stem cell mobilizer. The inducer composition for hematopoietic stem cells is useful for increasing the number of hematopoietic stem cells of a hematopoietic stem cell donor, and may be used for any donor of autologous hematopoietic stem-cell transplantation and allogeneic hematopoietic stem cell transplantation. In addition, the inducer composition for hematopoietic stem cells is also useful for treatment of conditions associated with a decrease in hematopoietic stem cells and treatment of patients undergoing chemotherapy or radiation therapy.
CA2321455C Indole-3-propionic acids, salts and esters thereof used as medicaments The cytotoxic effects of amyloid beta protein on cells are prevented by contacting the cells with an effective amount of an indole-3-propionic acid or a salt or ester thereof. Furthermore, a fibrillogenic disease can be treated in a human subject by administering to the human subject an amount of an indole-3-propionic acid or a salt or ester thereof effective to prevent or reverse fibrillogenesis. Oxidation in a biological sample can be decreased by contacting the biological sample with an effective amount of an indole-3-propionic acid or a salt or ester thereof. Additionally, diseases or other conditions where free radicals and/or oxidative stress play a role can be treated by administering an effective amount of an indole-3-propionic acid or a salt or ester thereof.
WO2014140597A1 2-((4-amino-3-(3-fluoro-5-hydroxyphenyl)-1h-pyrazolo[3,4-d]pyrimidin-1 -yl)methyl)-3-(2-(trifluoromet hyl)benzyl)quinazolin-4(3h)-one derivatives and their use as phosphoinositide 3-kinase inhibitors The present invention relates inter alia to a compound of formula (I) and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the said compounds.
CN1798559B Quinoline-2-one-derivatives for the treatment of airways diseases Compounds of formula (I) in free or salt form, wherein -C-Y-, R<1> and R<2> are G have the meanings as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the (beta2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
CN102030744A Iloperidone crystal and preparation method and medicinal composition thereof The invention provides an iloperidone crystal, which has X-ray diffraction peaks at 17.16 degrees, 20.68 degrees, 14.30 degrees, 16.74 degrees, 19.92 degrees, 20.30 degrees, 21.54 degrees, 22.10 degrees, 7.10 degrees, 12.64 degrees, 17.50 degrees, 18.20 degrees, 24.62 degrees, 25.12 degrees, 26.34 degrees, 28.92 degrees, 29.94 degrees, 30.72 degrees and 31.76 degrees represented by a 2theta anglein an X-ray diffraction pattern. The invention also provides a method for preparing the iloperidone crystal. The iloperidone crystal has a stable structure, can be stored for a long time, does not have any special requirement on temperature and humidity, and can be used for preparing a medicinal composition for treating schizophrenia.
WO2010093845A1 Triazole and imidazole derivatives for use as tgr5 agonists in the treatment of diabetes and obesity The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.
WO2007050720A1 Loteprednol etabonate against vascular dysfunction in the eye This invention relates to the effect of Loteprednol etabonate on vascular dysfunction in the back of the eye. More specifically, this invention relates to methods of modifying a pathogenic angiogenesis in the back of an eye of a patient, the method comprising administering to a patient in need thereof a pathogenic angiogenesis modifying amount of Loteprednol etabonate. Moreover, this invention relates to methods of modifying pathologic vascular permeability manifested as retinal edema. The method compromises administering to a patient an amount of LE sufficient to reduce retinal edema.
CN103585137A Paeonol lyotropic liquid crystal self-emulsified preparation and preparation method thereof The invention discloses a paeonol lyotropic liquid crystal self-emulsified preparation and a preparation method thereof. The paeonol lyotropic liquid crystal self-emulsified preparation comprises the following components in parts by weight: 2-10 parts of paeonol, 20-45 parts of a lyotropic liquid crystal material, 30-60 parts of an emulsifier and 10-25 parts of a co-emulsifier. The preparation method comprises the following steps: uniformly stirring and mixing the lyotropic liquid crystal material, the emulsifier and the co-emulsifier at the temperature of 37 DEG C, further adding a medicament, stirring, dissolving and uniformly mixing, standing and balancing for 24 hours at the temperature of 37 DEG C, cooling at room temperature so as to obtain the preparation. Through the preparation of the lyotropic liquid crystal into the self-emulsified preparation, the problem that the lyotropic liquid crystal is hard to orally taken because of the large viscosity is solved, the paeonol solubility is improved, and at the same time the effect of slowly releasing the medicament is achieved.
EP1311258B1 Compositions containing hypotriglyceridemically active stilbenoids The use of isolated or purified stilbenoid compounds including longistyline A-2-carboxylic acid as a dietary supplement to mammals suffering form elevated triglyceride levels is described. The invention also relates to the use of such stibenoid compounds in combination with other hypotriglyceridemic agents.
EP1439858B1 Use of granular materials based on pyrogenically produced silicon dioxide in pharmaceutical compositions The use of granular materials based on pyrogenically produced silicon dioxide in pharmaceutical compositions, the pharmaceutical compositions per se, as well as an adsorbate consisting of the granular material and at least one further substance selected from pharmaceutical active constituents and auxiliary substances, and the production of such adsorbates, are described.
WO2005018648A1 (20S)-1α-HYDROXY-2-METHYLENE-19-NOR-VITAMIN D3 AND ITS USES The compound (20S)-1 α-hydroxy-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor are described herein. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anticancer agent and for the tretment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
US20130052207 Prognostic Method for Pulmonary Adenocarcinoma, Pulmonary Adenocarcinoma Detection Kit, and Pharmaceutical Composition for Treating Pulmonary Adenocarcinoma A method of detecting a poor-prognosis stage I lung adenocarcinoma in a mammal, comprising a step of measuring the copy number of ACTN4 gene in the cells of the stage I lung adenocarcinoma tissue obtained from the mammal, wherein, when the copy number of the gene exceeds 4, the stage I lung adenocarcinoma in the mammal is predicted to be a poor-prognosis stage I lung adenocarcinoma.
US7037926 Anticarcinogenic, antiallergen, and antiinflammatory agents; autoimmuned diseases Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.
US20080089910 Attenuated Herpes Simplex Virus Type-2, Vectors Thereof and Immunogenic Compositions Thereof The present invention broadly relates to the attenuation of herpes simplex virus type 2 (HSV-2). More particularly, the invention relates to the identification of mutations in the HSV-2 UL24 gene which attenuate the pathogenicity of HSV vectors in mammals and immunogenic compositions thereof.
US7354610 Phospholipid complexes of standardized vegetable extract of Vitis vinifera and of standardized vegetable extract of Centella asiatica; may also include vitamin E, zinc, hydroxyacids, or glycyrrhetinic acid or its complex with phospholipids; does not contain fish cartilage extract Pharmaceutical and cosmetic compositions for the prevention of skin aging, containing phospholipid complexes of extracts of Vitis vinifera, and phospholipid complexes of standardized extract from Centella asiatica.
CN102357074A Anti-tumor multi-medicine resistant targeted liposome The invention relates to an anti-tumor multi-medicine resistant targeted liposome and a preparation method thereof, in particular to an anti-tumor multi-medicine resistant long circulating targeted liposome. The invention is characterized in that: quercitin and an anti-tumor medicine are jointly coated in the liposome, and simultaneously target tumor tissues to reverse the multi-medicine resistance of tumors, cytotoxicity of anti-tumor medicines on medicine resistant tumors is enhanced, the change of pharmacokinetic properties of the anti-tumor medicines in vivo and the enhancement of toxic and side effects of the anti-tumor medicines in vivo, which are caused by the difference and interaction of the pharmacokinetic properties of different medicines in vivo, are avoided, and the treatmenteffect on medicine resistant tumors is improved.
CN101787007B Dimeric sesquiterpene compound and applications thereof The invention provides a dimeric sesquiterpene compound, a preparation method thereof and the applications in aspects of angiogenesis inhibition, anti-prolyl endopeptidase, antibiosis, apastia and spice by using the compound as an active component.
US20110076306 Arabinogalactan for enhancing the adaptive immune response The present invention discloses a composition containing Arabinogalactan for enhancing the adaptive immune response in subjects to foreign antigen(s) by administering said composition prior, during and after the phase of exposure to said foreign antigen(s). Furthermore, the present invention relates to a vaccination kit comprising a composition comprising Arabinogalactan and a vaccine.
CN101543490A Application of genistein in medicament preparation for treating hyperplasia of prostate, product and producing method The invention discloses an application of the genistein in the medicament preparation for treating hyperplasia of prostate, a product and a producing method. The medicament for treating benign hyperplasia of prostate is prepared by 1-50 portions by weight of genistein and 1-50 portions by weight of zedoary turmeric oil. Compared with the prior technology, the invention applies the genistein to the medicament and the health products for treating hyperplasia of prostate, broadens the application range of the genistein and reasonably combines the genistein with the zedoary turmeric oil to obtain a good medicament preparation for treating hyperplasia of prostate with exact treating effect, rapid acting and little toxic and side effects.
US20070009600 Antidepressant dosage form The invention pertains to a dosage form 10 and to administering an antidepressant medicament 16 for an extended period of time in a rate-known dose.
WO2007138072A3 Triazolopyrazine compounds useful for the treatment of degenerative & inflammatory diseases Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following (formula I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.
CN102727443A Clathrate of mesoporous silicon oxide/Fe3O4 magnetic nano-grade complex and ibuprofen The invention discloses a clathrate of a mesoporous silicon oxide/Fe3O4 magnetic nano-grade complex and ibuprofen. The clathrate is prepared through the steps that: the mesoporous silicon oxide/Fe3O4 magnetic nano-grade complex is added into an ibuprofen ethanol solution, wherein the mass ratio of ibuprofen to the mesoporous silicon oxide/Fe3O4 magnetic nano-grade complex is 1:0.25-25; the mixture is subjected to ultrasonic treatment for 2-5h; an obtained product is washed by using twice-distilled water; the product is separated by using a permanent magnet; the obtained product is subjected to vacuum drying for 6-8h under a temperature of 50-70 DEG C, such that a solid clathrate is obtained. The clathrate can be used for preparing an ibuprofen targeting medicine. Under the effect of an external magnetic field, the contained medicine can be released at the exact position of a lesion site. Therefore, medicine adverse reactions can be reduced, administration frequencies can be reduced, and medicine maximal curative effect can be developed.
CN1640401A Tetrandrine preparation foreyes The present invention discloses a kind of tetrandrine eye preparation. It is an anti-inflammatory drug for curing eye disease, and includes liquid or ointment body excipient of eye preparation. Its composition includes (wt%) 0.01-2% of tetrandrine and 98-99.99% of excipient. The tetrandrine eye drops prepared by said invention can be made up by using tetrandrine, anti-oxidant, metal ion complexant, osmotic pressure regulating agent, bacteriostatic agent, cosolvent, thickening agent, keratolytic agent and injection water. Said invention also provides tetrandrine eye ointment and tetrandrine gel type eye ointment.
CN102846567A Preparation of xanthan gum vildagliptin intragastric retentive floating sustained-release tablet The invention relates to the field of medicinal preparations, and particularly relates to a preparation method of a xanthan gum vildagliptin intragastric retentive floating sustained-release tablet. Vildagliptin is a derivative of cyanopyrrolidine, and is an effective and reversible specific competitive dipeptidyl peptidase IV inhibitor. Common adverse reactions of vildagliptin comprise headache, hypertension deterioration and the like. Substrates degraded by DPPIV is extensive, so the DPPIV inhibitor has potential effect on blood pressure, immune system, and the like; and the drug has a short half life, so new technology is necessary to the increase of the period with an effective drug concentration, the increase of bioavailability, and the reduction of side effect. The invention adopts xanthan gum as a skeleton, and some additives are added to facilitate the decrease of the preparation density, and the prevention of skeleton hydration. The invention mainly solves the problems of release speed control, drug release from the skeleton by a corrosion mechanism, and optimization of prescription drug release characteristics to meet an Higuichi equation, and thus increases the bioavailability and prolongs the action time.
CN103463127A Sodium acetate ringer injection and preparation method thereof The invention discloses a sodium acetate ringer injection. The preparation method of the injection comprises the following steps of: adding 60-80 percent by prescription of fresh injection water into a preparation tank, stirring and adding 100 percent by prescription of a sodium acetate ringer component; dissolving, and adding the injection water to 100 percent of the prescription, stirring, and regulating the pH value to 7.0-7.5; starting a liquid medicine pump to circulate a liquid medicine sequentially in a 5mu m filter element, a 0.45mu m filter element and a reflux pipeline; inspecting whether a sample is qualified, filtering the liquid medicine through filter elements of 10mu m, 0.45mu m and 0.2mu m, canning and sterilizing. The preparation method does not use activated carbon, so that the influence of the activated carbon to medicine quality and environmental pollution can be avoided, the sterilization condition can be improved, and the sterile level of medicines can be better guaranteed; furthermore, the production operation is simpler, the preparation time is shortened, and the production cost is saved.
US20080293808 Non-Steroidal Androgen Receptor Modulators, Preparation Process, Pharmaceutical Composition and Use Thereof Non-steroidal androgen receptor modulating compounds of the general formula (I), their pharmaceutically acceptable salts, preparation process and pharmaceutically compositions containing the said compounds are disclosed. Such compounds of the general formula (I) or their pharmaceutically acceptable salts can be used for preparing non-steroidal medicines to treat and/or prevent conditions or diseases such as prostatic hyperplasia, prostate cancer, hirsutism, severe hormone-dependent alopecia or acne, etc. as a result of androgen receptor antagonistic activities.
CN1861083A Compound medicine for treating migraine headache A compound medicine for treating hemicrania is proportionally prepared from aspirin, caffeine, indometacin and cortal.
CN102641249A Preparation method of tigecycline composition The invention relates to a preparation method of tigecycline composition, which comprises enabling lactose to be dissolved by using 80% water for injection, conducting ultrafiltration treatment on lactose solution, collecting ultrafiltrate, adding tigecycline after the solution is cooled, evenly mixing, adjusting the potential of hydrogen (pH) value to 4.0-6.0, adding activated carbon for a needle for stirring, adsorption and decarburization, and conducting constant volume; enabling the solution to be filled in a penicillin bottle after filtration, conducting semi-plugging, disc loading, freeze-drying, nitrogen communicating, plug pressing, outbox and cover rolling, packaging after quality testing is qualified, and then obtaining the tigecycline composition. The protein concentration of the composition obtaining through the preparation method is smaller than 0.005g/L, untoward effects caused by the fact that lactose is added in the products are greatly reduced, the preparation method is simple and convenient in operation and low in cost, and prepared products are good in quality and easy in industrial production.
CN103087042A Salts of sitafloxacin and pharmaceutical purposes thereof The invention provides acid addition salts of sitafloxacin represented by the formula, crystal forms and preparation methods of the salts, and pharmaceutical compositions, preparations and pharmaceutical purposes of the salts, wherein A is described in the specification. Both stability and water-solubility of the salts of the sitafloxacin or the crystal forms are better than that of sitafloxacin free alkali; furthermore, the irritation is less than that of the sitafloxacin free alkali; and the compositions or preparations prepared from the salts are applied to clinical applications.
US20080108600 Polycyclic Pyridines as Potassium Ion Channel Modulators The present invention provides a genus of polycyclic pyridines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.
CN103622991A Synergistic diluent for root canal washing fluids and preparation method therefor The invention relates to the medical technology field, and discloses a synergistic diluent for root canal washing fluids and a preparation method therefor. The synergistic diluents is packaged with a common enclosed container, and used for dilution, toxicity attenuation and synergy of root canal washing fluids in common use ( such as sodium hypochlorite solution, hydrogen peroxide solution and the like). The diluent mainly contains safe synergist amino acids, isoosmotic adjusting agents, gel thickening agents, alkaline pH conditioning agents, food colourings and/or essences and the like. The synergistic diluent can lower the damage of root canal washing fluids to oral mucosae obviously, the toxicity of the root canal washing fluids can be reduced, the peculiar smell of the root canal washing fluids can be eliminated, and the synergistic diluents is suitable for clinical application of dentistry.
CN101905007A Plaster for curing rheumatoid pains in neck, shoulders, waist and legs The invention discloses a plaster for curing rheumatoid pains in a neck, shoulders, a waist and legs, which is prepared from the following raw materials by weight: musk, radix notoginseng, ligusticum wallichii, lycopodium clavatum, garden balsam stem, red flower, processed radix aconiti kusnezoffii, processed radix aconiti, radix clematidis, processed semen strychni, frankincense, myrrh, asarum, radix angelicae pubescentis, pawpaw, curcuma zedoary, rhizoma sparganii, Chinese angelica, borneol and decumbent corydalis tuber. The plaster has the effects of promoting blood circulation, removing blood stasis, relaxing tendons, activating collaterals, dispelling wind, removing heat, resolving hard lump and relieving bruises and pains; when the plaster of the invention is coated on a fracture and reduced joint after fracture and reduced joint integration, local revascularization can be improved, and porosis is generated quickly; the plaster has good recovery effects on sequelae such as pains, joint swelling, inconvenient activity, stiffness and the like caused by the plaster immobilization and dermatoplasty; and the medicament of the invention has the advantages of simple preparation process, convenient using method, safety, no side effect, obvious curing effect and high efficiency.
CN101428029A Uses of curcurbitacin in producing medicament for treating cancer The invention relates to new application of dihydrocucurbitacin F-25-O-acetate in preparation of medicines for treating cancer. The invention also relates to the application of dihydrocucurbitacin F-25-O-acetate in preparation of medicines for treating leucocythemia.
US20130177599 Methods and kits for extending contact lens use Provided are method and kits useful for extending the wear-time of a contact lens. The method includes applying an amount of an ophthalmically acceptable solution to the contact lens to improve the comfort of the eye when the contact lens is in the eye. The solution includes an aqueous suspension and chitosan. The aqueous suspension includes about 0.1% to about 6.5% by weight of a carboxyl-containing polymer prepared by polymerizing one or more carboxyl-containing monoethylenically unsaturated monomers and less than about 5% by weight of a cross-linking agent. Upon contact with tear fluid, the solution gels to a second viscosity which is greater than the first viscosity. The kit includes contact lenses, an ophthalmically acceptable solution and instructions for applying the solution to improve the comfort of the eye when the contact lens is in the eye.
CN103733069A Method of screening for chaperonin modulator The present invention relates to a method of screening for modulator of chaperonin that is involved in protein aggregation inducing neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, use of the chaperonin modulator screened by the method for prevention and treatment of neurodegenerative diseases. According to the present invention, novel negative chaperonin modulator is provided, and chaperonin modulator may be more rapidly and conveniently screened with the negative modulator as a target. Furthermore, by using the screened material, neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease may be effectively prevented or treated without concern for cell death due to autophagy, which is the existing method of removing protein aggregate.
US20110224203 Benzimidazole derivatives and their use as protein kinase inhibitors The invention provides compounds of the formula (I): The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Aurora kinases and are therefore useful to treat cancer and viral diseases.
EP1212000B1 System for controlling body temperature while reducing shivering This invention is using a heat exchange device (240) in combination with an anti-shivering mechanism that temporarily reduces shivering for lowering the body temperature of a patient. Various anti-shivering agents are disclosed including dopamine receptor blockers, dopamine receptor agonists, opioid agonist antagonist analgesics, serotonin 5 HT1a agonists, and pharmaceutically acceptable salts of any members of this group.
EP1948167A1 Compositions of phosphodiesterase type iv inhibitors Provided herein are pharmaceutical compositions comprising one or more phosphodiesterase inhibitors of type IV ('PDE-IV'), and at least one other active ingredients selected from muscarinic receptor antagonists (MRA), ß2-agonists, p38 MAP Kinase inhibitors, and corticosteroids and optionally one or more pharmaceutically acceptable excipients and/or other therapeutic agents. In addition, methods of treating autoimmune, inflammatory or allergic diseases or disorders are provided.
US20120094953 Process for the production of nano-fibrillar cellulose suspensions The present invention relates to a process for the production of suspensions of nano-fibrillar cellulose by providing cellulose fibres and at least one filler and/or pigment; combining the cellulose fibres and the at least one filler and/or pigment; and fibrillating the cellulose fibres in the presence of at least one filler and/or pigment, as well as the suspensions of nano-fibrillar cellulose obtained by this process and their uses.
CN102488697A Application of oligomeric mannuronic acid to preparation of medicine for resisting influenza A virus subtype H1N1 The invention provides application of oligomeric mannuronic acid to preparation of a medicine for resisting influenza A virus subtype H1N1. Through experiment, the oligomeric mannuronic acid (OM) has a good function of protecting madin-darby canine kidney cells which are infected by influenza A virus subtype H1N1 in vitro, can effectively reduce virus reproduction, and has an effect equal to thatof a positive control medicine ribavirin. Moreover, OM can also reduce the death of mice which is caused by infection of influenza A virus subtype H1N1 obviously, and prolong the survival time. The oligomeric mannuronic acid (OM) has the advantages of high water solubility and stability, and safety and low toxicity and the like; and in an in vivo-in vitro experiment, the OM can resist influenza Avirus subtype H1N1 well, and the oligomeric mannuronic acid can be expected to be developed to the medicine for resisting influenza A virus.
CN101680002B A series of recombinant adeno-associated viral vectors, construction methods and uses thereof A series of recombinant adeno-associated viral vectors (rAAVs), construction methods and uses thereof are disclosed. Each one of the rAAVs is obtained by replacing adeno-associated virus structure gene with one of the following tumor antigen genes: PSA, PSMA, CEA, CK19, Her-2/neu, LMP-1, BA46 or AFP, or mutant type of each gene, respectively. Each one of the rAAVs of the present invention can deliver its carried wild-type or mutant prostate specific antigen gene into monocyte-macrophage-dendritic cell lines to stimulate effector cells of immune system. It has been experimentally showed that CTL induced by DC, which is infected with one of the rAAVs of the present invention, can effectively inhibit the growth of malignant tumor cells or kill tumor cells in vivo in patients. The recombinantadeno-associated viral vectors of this invention and their related products can be used to prepare the medicaments for the treatment of prostatic cancer, epithelial cell malignant tumor, breast cancer, colon cancer, stomach cancer, adenocarcinoma of lung, lung cancer, oophoroma, nasopharyngeal carcinoma, cervical carcinoma, squamous carcinoma of lung, liver cancer, etc.
WO2007022042A3 Combinations comrising a protein kinase inhibitor being a pyrimidylaminobξnzamide compound and a hsp90 inhibitor such as 17-aag The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound; and b) an HSP90 inhibitor, and a method for treating or preventing a proliferative disease using such a combination.
US7273877 5-substituted-4-[(substituted phenyl) amino]-2-pyridone derivatives The present invention relates to 5-substituted-4-(substituted)phenylamino-2-pyridone derivatives, pharmaceutical compositions and methods of use thereof.
US7560464 (5-Methoxy-2-pyridin-2-yl-pyrimidin-4-yl)-(5-pyrrolidin-1-yl-pyridin-2-yl)-amine; SK channel modulators (SK=small conductance calcium activated potassium channels); antiepileptic agents; seizures; learning enhancement; cognition activators; mood/psychotic disorders; antidepressants; Parkinson's disease The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.
WO2006038656A1 Allergy suppressant It is intended to provide a novel agent/composition wherein a bioregulatory function of a food component is utilized. Namely, an allergy suppressant containing chrysin, more specifically speaking, a histamine release inhibitor containing chrysin; a composition containing chrysin which is to be used in treating a disease or conditions relating to IgE production; a composition containing chrysin which is to be used in treating a disease or conditions relating to an IgE receptor with a high affinity; and a composition containing chrysin which is to be used in treating a disease or conditions relating to the overproduction of IL-4. It is preferable that the allergy suppressant, the histamine inhibitor or the composition as described above further contains apigenin.
WO2011127499A1 Animal feed additive having an antimicrobial and growth-promoting effect The invention relates to an animal feed additive having an antimicrobial and growth-promoting effect, characterized in that the animal feed additive contains a material, which contains lignocellulose and which binds iron ions, in combination with a plant antimicrobial active ingredient. Especially advantageous materials containing lignocellulose and binding iron ions are obtained from the group of the Pinus species, the plant antimicrobial active ingredient preferably being obtained from plants of the Magnolia genus or the Cinnamomum genus.
CN1765934A Nanometer mushroom amylose and preparation method of its injection The invention discloses a preparation method for nano lentinan and its injection. Wherein, to the injection, using mushroom body as material, preparing nano mushroom by microwave extracting and supersonic jet, extracting lentinan, and generating injection or freeze-drying to powder injection with excipient. Compared with prior art, this product has simple scientific process, high yield and purity.
WO2013104540A1 New c5a binding nucleic acids The present invention is related to a nucleic acid molecule capable of binding to human C5a, wherein the nucleic acid molecule comprises a central stretch of nucleotides, wherein the central stretch of nucleotides comprises a nucleotide sequence of 5' AUGn1GGUGKUn2n3RGGGHUGUKGGGn4Gn5CGACGCA 3' [SEQ ID NO: 61], wherein n1 is U or dU, n2 is G or dG, n3 is A or dA, n4 is U or dU, n5 is U or dU and G, A, U, C, H, K, and R are ribonucleotides, and dU, dG and dA are 2'-deoxyribonucleotides.
CN103127124A Medicine composition of selegiline and folic acid type compound and use thereof The invention relates to a medicine composition of selegiline and a folic acid type compound and use of the medicine composition of the selegiline and the folic acid type compound and belongs to the technical field of pharmacy. The medicine composition comprises the selegiline of medicinal dose, the folic acid type compound of medicinal dose and a carrier capable of being accepted by the pharmacy. The dose of the selegiline is 5 milligrams to 10 milligrams. The dose of the folic acid type compound is 0.2 milligram to 1.6 milligrams. The medicine composition of the selegiline and the folic acid type compound and the use of the medicine composition of the selegiline and the folic acid type compound has the advantages of increasing curative effect of Parkinson disease resistance through synergistic effect of multiple-target, improving life quality of a patient, effectively preventing and reducing occurrence risk of cerebral apoplexy of the patient with the Parkinson disease through a homocysteine (Hcy) target, and additionally enabling the patient to conveniently take medicine.
CN102228442A Star-like macromolecule nanometer microsphere and preparation method and application thereof The invention discloses a star-like macromolecule nanometer microsphere, which takes 5,10,15,20-tetra(4-aminophenyl) porphyrin or dipyridamole as a kernel and is characterized in that the surface of the nanometer microsphere is hydrophilic polyethylene and the interior of the nanometer microsphere is hydrophobic epsilon-caprolactone. The molecular weight of the macromolecule nanometer microsphereis 30000-50000, the molecular weight of the hydrophilic is 5000*4; the molecular weight of the hydrophobic part is 10000-30000; and the average particle size of the nanometer microsphere is 20-60 nm.In the invention, the compound nanometer microsphere has good biocompatibility and stable chemical property. The star-like macromolecule nanometer microsphere can be used as a drug carrier, has a function of slow release and further can be used for fluorescence labelling. The invention also discloses a preparation method and an application of the star-like macromolecule nanometer microsphere.
US7153502 Food or drink product with a disinfection property of Helicobacter pylori A food or drink product with a disinfection property of Helicobacter pylori and/or a protection property against infection with H. pylori, comprising as the effective ingredient Lactobacillus gasseri OLL 2716 (FERM BP-6999) with a high disinfection potency of H. pylori. The food or drink product prepared by using the lactic acid bacterium, such as acid milk and the like, is suitable for long-term ingestion as a food or drink product with a disinfection property of H. pylori and/or a protection property against infection with H. pylori.
US7381739 Antiserotonine agents; central nervous system disorders; Alzheimer's disease; Parkinson's disease; Huntington's disease; sleep disorders The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, p and n are those defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.
US7820671 Peptidomimetic protease inhibitors The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
EP0907735B2 Modulators of tissue regeneration Proteins which are upregulated in injured or regenerating tissues, as well as the DNA encoding these proteins, are disclosed, as well as therapeutic compositions and methods of treatment encompassing these compounds.
CN101822836A Medicine composition containing allisartan isoproxil The invention relates to a medicine composition containing allisartan isoproxil or pharmaceutically acceptable salts thereof, at least one cardiovascular and cerebrovascular medicine and pharmaceutically acceptable vectors. The composition is used for preventing, slowing the progress of or treating the following diseases or symptoms of: hypertension, hypertension complications, diabetes, diabetes complications, dyslipidemia, ischemic diseases, coronary heart disease, angina, cardiac arrhythmia, stroke, arteriosclerosis, cerebral infarction, cerebral vascular diseases, cardiovascular diseases, coronary artery diseases, ventricular dysfunction, endothelial dysfunction, heart insufficiency, glaucoma and cataract, reducing the incidence and/or the mortality of cardiovascular and cerebrovascular diseases, decreasing the side effects, and also improving the medication compliance of patients.
US20080317717 Anti-hepatitis b virus ribozymal nucleic acid This invention relates to ribozymes which cleave Hepatitis B Virus (HBV) at CUC sites. Suitable ribozymes may, for example, cleave at GGCUCUCUCGUCCC, CCUCAGCUCUGUAUCG or GAGGACUCUUGGA recognition sequences in HBV RNA. Ribozymal DNA, vector systems and pharmaceutical compositions are provided which may be useful, for example, in the treatment of HBV infection.
US20090082380 Deuterium-enriched rosuvastatin The present application describes deuterium-enriched rosuvastatin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN101306009A Function food for protecting nourishing the liver The invention discloses a functional food for protecting and nourishing a liver, which comprises the active ingredients by the weight percentages as follows: 5 to 75 percent of alginate, 10 to 80 percent of taurine and 15 to 85 percent of L-arginine. In the active ingredients of the functional food, the alginate has the function of regulating the liver immune system, the taurine has the detoxification function, and the L-arginine has the functions of relaxing the blood vessels and increasing the blood flow volume. The functional food combines the functions of the alginate, the taurine and the L-arginine according to a certain rule, and manufactures the functional food according to a certain component proportion, thereby leading the alginate, the taurine and the L-arginine to be put into full-play during the process of protecting and nourishing the liver, and achieving the purpose of effectively protecting and nourishing the liver.
CN102512425A Preparation method of inclusion compound of ursolic acid and schardinger dextrin The invention relates to a preparation method of an inclusion compound of ursolic acid and schardinger dextrin, which comprises the following steps of: mixing an ethanol solution of ursolic acid and a water solution of schardinger dextrin, wherein the mol ratio of the ursolic acid and the schardinger dextrin is 1:1 to 10; placing a mixed solution into a homogenizing machine with ultra-high pressure and homogenizing for at least one time at 100 to 200MPa; and placing a homogenized solution into a water bath at 55 DEG C and concentrating in a decompression way until the solution is in a semitransparent thick shape so as to obtain a powdery product after drying obtained concentrated liquid; and the preparation method of the inclusion compound of the ursolic acid and the schardinger dextrin has the technical effects that the time is short, the destruction of the schardinger dextrin is little, and the aim of continuous preparation can be achieved.
US7341700 Method for recovery of metals from metal-containing materials using medium temperature pressure leaching The present invention relates generally to a process for recovering copper and other metal values from metal-containing materials using controlled, super-fine grinding and medium temperature pressure leaching. Processes embodying aspects of the present invention may be beneficial for recovering a variety of metals such as copper, gold, silver, nickel, cobalt, molybdenum, rhenium, zinc, uranium, and platinum group metals, from metal-bearing materials, and find particular utility in connection with the extraction of copper from copper sulfide ores and concentrates.
US20080114030 Diarymethyl and related compounds This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
US20070031507 Bactericide for MRSA A bactericide for MRSA and a method for making the bactericide are disclosed. The bactericide is characterized in that it comprises a product prepared by pulverizing a shell having a crystalline structure of a calcite structure of calcium carbonate. The bactericide allows a wide variety of articles to be sterilized by the use of one type of bactericide, which leads to simplification of the management of chemicals for use in sterilization and learning of methods for using them and thus to saving in work.
CN102048847A Externally applied medicine for treating frostbite The invention relates to a formula of soaking solution for treating frostbite, which belongs to the field of sanitation and daily chemicals. The soaking solution is characterized by being prepared from mulberry twig, cassia twig, liquoric root and the like. The formula comprises 80-150g of the mulberry twig, 30-60g of the cassia twig, 20-50g of the liquoric root, 10-40g of golden thread, 3-7g of white spirit and 1-3g of edible salt. The soaking solution is not only sanitary, but also convenient to use, thus the formula of the soaking solution is more practical and faster in curative effect.
US8318790 Heat Shock Protein 90 (HSP90); treating cancer, inflammatory disorders, angiogenesis inhibition, infections; 3-substituted-4-fused(hetero)aryl-5-phenyl-4H-1,2,4-triazoles The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
CN101455673B Use of cinnamyl-(6'-O-alpha-L- arabopyranose)- O-beta-D-glucopyranoside in preparing antidepressant medicine The invention relates to applications of a compound cinnamyl-(6'-O-alpha-L-arabopyranose)-O-beta-D-glucopyranoside in pharmaceutical field. The compound can effectively resist blepharoptosis caused by reserpine or akinesia, resist small mouse thrill caused by L-5-HT, resist small mouse tail suspension or acquired desperation depression by a forced swinging method, strengthen L-dopa behavioural effect, and has no exciting or inhibiting effect to nerve centres. The action mechanism thereof may be related to breaking reuptake of NA, DA transmittances so as to increase concentration of the two transmittances in synaptic spaces. The compound has no toxic reactions in acute toxicity experiences on mice so that the compound with experience dosage has relatively high security and good anti-depression effect and can be used to treat depression.
WO2014016433A1 Derivatives of azaindazole or diazaindazole type for treating pain The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; for use in the treatment of pain.
US7074420 Cosmetic treatment using a new retinoid There is provided a topical composition and method for improving the aesthetic appearance of skin, particularly, preventing, ameliorating, treating and/or reducing fine lines and/or wrinkles, without the skin irritation typically associated with topical application of a retinoid. There is also provided a topical composition and method for improving the aesthetic appearance of lips, particularly decreasing the number and/or depth of vertical lip lines. The composition has an effective amount of retinoxytrimethylsilane. Preferably, the composition is applied daily to skin and/or lips. The composition and method are particularly suitable for persons having sensitive skin.
US20090226538 Anticancer or antiviral composition Disclosed is an anticancer or an antiviral composition comprising therapeutically effective amounts of citric acid and or zinc and L-arginine along with a pharmaceutically acceptable carrier. The anticancer composition of the present invention has a strong anticancer effect while not having harmful side effects. The antiviral compositions of the present invention is useful for treatment of diseases caused by viral infections.
US20100279986 Heterocyclic derived metalloprotease inhibitors This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
CN101185623A Mycophenolate mofetil dry suspension agent The invention discloses a mycophenolate mofetil dry suspension, which consists of the following components and contents (weight unit): 125-600 portions of mycophenolate mofetil, 400-1000 portions of loading agents, 10-60 portions of sweetening agents, 50-100 portions of suspending agents, and appropriate quantity of wetting agents. The dry suspension has the advantages of easy administration, large production, easy quality control and convenient administration of patients.
WO2010044390A1 Viral infection therapeutic drug containing polyalkyleneimine Provided is a viral infection therapeutic drug having a mode of action that is different from conventional antiviral drugs and thereby inhibits the appearance of drug-resistant viruses. When a polyalkyleneimine having a pre-determined molecular weight is administered to a living body, the polyalkyleneimine is adsorbed by the virus that has invaded the living body and the virus is prevented from being adsorbed by cells or from invading cells. As a result, the virus is deactivated and the viral infection is thereby treated or prevented.
EP1420790B1 Use of bibn4096 in combination with other antimigraine drugs for the treatment of migraine The present invention relates to a method of treatment or prevention of headache, migraine or cluster headaches, which method comprises co-administration of a therapeutically effective amount of the compound A = 1-[N2-[3,5-Dibromo-N-[[4-(3,4-dihydro-2(1 H)-oxochinazolin-3-yl)-1-piperidinyl]-carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine [BIBN4096BS] or a physiologically acceptable salt thereof and a therapeutically effective amount of a second active antimigraine drug, particularly sumatriptan, zolmitriptan or dihydroergotamin or a physiologically acceptable salt thereof, as well as to the corresponding pharmaceutical compositions and the preparation thereof.
EP2167098A1 Allopregnanolone in a method for enhancing neurological function (alzheimer disease) Neuro-enhancing agents, compositions and methods are disclosed herein. Preferred neuro-enhancing agents of the present invention include progesterone and metabolites of progesterone, such as 3α-hydroxy-5α- pregnan-20-one (THP). These agents yield neuro-enhancing effects on neural cells that include neural progenitor and/or stem cells, whereby the agents stimulate mitosis of neural progenitor cells, stimulate neurite growth and organization, protect against neural loss, or one or more of these neural processes. Thus, the neuro-enhancing agents, compositions and methods disclosed herein are useful to reverse or prevent neurological disease or defects associated with neural loss or degeneration., such as Alzheimer's disease, neurological injuries, including injuries resulting from radiation therapy, and age-related neurological decline, including impairments in memory and learning.
US20120277260 Use of methylnaltrexone and related compounds to treat constipation in chronic opioid users A method of preventing or treating constipation in a patient who has been chronically taking opioids, the method comprising administering a quaternary derivative of noroxymorphone in an amount sufficient to prevent or treat the side effect in the patient, but which amount would be insufficient to treat a patient with the same opioid-induced side effect who had not chronically been administered opioids.
WO2006058121A1 Crystalline forms of 3'-tert-butyl-3'-n-tert-butyloxycarbonyl-4-deacetyl-3'-dephenyl-3'-n-debenzoyl-4-o-methoxycarbonyl-paclitaxel The present invention relates to crystalline forms of 3’-tert-Butyl-3’-N-tert-butyloxycarbonyl-4-deacetyl-3’-dephenyl-3’-N-debenzoyl-4-O-methoxycarbonyl-paclitaxel represented by formula (I); processes for the production thereof ; methods for preparing the pharmaceutical composition ; and methods for inhibiting tumor growth therewith.
CN103599113A Composition for supplementing calcium and zinc The invention relates to a composition for supplementing calcium and zinc. The composition contains stachyose, zinc gluconate, calcium citrate malate, vitamin K and vitamin D, wherein the content of stachyose is 5-60 mg, the content of calcium citrate malate is 20-80 mg, the content of zinc gluconate is 1-10 mg, the content of vitamin K is 1-2.5 mg, and the content of vitamin D is 3.7-12.5 mg.
WO2012058526A1 Inhibition of microbial growth by aconitase inhibition The present invention is directed to a method of inhibiting aconitase activity of fungal cells in an individual, the method comprising administering an inhibitor of aconitase activity to the fungal cell in an amount effective to inhibit activity of aconitase by said fungal cells.
CN103739656A 28-O-beta-D-glucosyl phytolaccagenin, and preparation method and application thereof The invention relates to the field of biological medicines, and particularly discloses a 28-O-beta-D-glucosyl phytolaccagenin (I) and a preparation method thereof by biotransforming phytolaccagenin by a strain with the collection number of NRRL1086. The invention also discloses application of the 28-O-beta-D-glucosyl phytolaccagenin in the anti-inflammatory aspect.
WO2008018089A1 R-(-) / s-(+)-7-[3-n-substituted amino-2-hydroxypropoxy] flavones The present invention provides an optically active compound of general formula (I) and salts thereof: wherein R' is selected from a group consisting of t-butyl amine, n-butylamine, iso- butylamine, iso-propyl amine, 4-phenyl-piperazine-1-ylamine, 4-(2-methoxyphenyl)- piperazin-1-ylamine, and 3, 4-dimethoxy phenethyl amine; wherein R1, R2 and R3 are selected from the group consisting of hydrogen, methyl or iso pentenyl; R4, R5 and R6 are selected from the group consisting of OH, O-alkyl, O-benzyl, O-substituted phenyl or combination thereof.
WO2009086097A1 Intraocular irrigating solutions comprising histidine and methods for treating corneal edema One aspect of the present invention relates to methods of treating corneal edema comprising contacting a cornea with an ophthalmic irrigating composition comprising histidine. In certain embodiments, the ophthalmic irrigating compositions contact the corneal endothelium. Another aspect of the present invention relates to ophthalmic irrigating compositions for treating corneal edema comprising histidine and optionally, calcium glycerophosphate and/or glutathione disulfide.
US20070282012 Reagent for Lacrimation Examination and Method of Lacrimation Examination A new application of the dacryogenic component of onions and analogues of the component in the medicinal field. It is a reagent for lacrimation examination which contains as an active ingredient a compound represented by the following chemical formula: wherein R represents a C1-5 alkyl chain.
CN102153613A Method for preparing prunellin and application The invention discloses a method for preparing prunellin and application, in particular a method for preparing the prunellin by taking ursolic acid as a raw material and structurally modifying the ursolic acid and product application thereof. 1alpha,2alpha-dyhydroxy ursolic acid (namely the prunellin) is prepared by the scientific and reasonable method; in the method, reaction conditions are mild, special instruments and equipment are not needed, the operation is simple and easy, scale can be enlarged and the aim of industrialized production is fulfilled easily; moreover, the prunellin prepared by the method and salts (sodium salt, potassium salt or ammonium salt) thereof have a remarkable effect of preventing hepatocyte injury caused by CCl4, have high activity for preventing mouse liverinjury caused by the CCl4, and can be taken as a liver protection medicament to be applied to the preparation of medicaments for acute and chronic hepatitis and related diseases of hepatic impairmentcaused by alcohol, chemical substances or medicaments.
US20100305147 Chemically modified small molecules The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer.
CN102973649A Throat-clearing emulsion and preparation method thereof The invention discloses a throat-clearing emulsion and a preparation method thereof. The preparation method comprises the following steps: performing aqueous extraction to myrobalan, filtering and concentrating to obtain a first paste, performing alcohol precipitation, and recycling ethanol to obtain a myrobalan paste; taking indigo naturalis, adding hydrochloric acid aqueous solution to dip, washing until the aqueous solution is neutral, and drying to obtain refined indigo naturalis; adding water to extract the liquorice, filtering, concentrating to obtain a second paste, adding ethanol into the second paste, standing, taking supernatant, adjusting the pH, filtering, recycling ethanol from filtrate, adding water, adjusting pH, filtering, using water to wash precipitation, and drying to obtain liquorice extractive; drying and smashing the myrobalan paste, evenly mixing the myrobalan paste, the smashed refined indigo naturalis, calculus bovis factitius, borneol, menthol and liquorice extractive to obtain a mixture, adding oil and emulsifying agent in the mixture to evenly mix to obtain an oil phase, taking an auxiliary emulsifying agent, adding water to dissolve the auxiliary emulsifying agent, adding the mixture of water and the auxiliary emulsifying agent into the oil phase to emulsify, adding an antioxidant, using a colloid mill to emulsify, filtering, sealing in a pot, and sterilizing. The throat-clearing emulsion does not contain sugar, is low in cost, safe, good in treatment effect and convenient to carry. The work time is less, and the transport rate of effective ingredients is high.
CN101602730A Substituted imidazole derivative The invention provides a new substituted imidazole derivative having structure of formula (I), also provides a pharmaceutical composition including the compound and applications of the compound and the composition. The compound of the invention can be used for inhibiting tubulin and neovascularization.
US20080132464 Selective induction of apoptosis to treat ocular disease The invention is directed to a method of prophylactically or therapeutically treating choroidal neovascularization, wherein the method comprises directly administering to the eye a therapeutic factor or a nucleic acid sequence that encodes a therapeutic factor, which he expressed to produce the therapeutic factor, to selectively induce apoptosis of endothelial cells associated with neovascularization of the choroid such that choroidal neovascularization is treated prophylactically or therapeutically. The invention also provides a method of prophylactically or therapeutically treating ocular neovascularization, wherein the method comprises directly administering to the eye a nucleic acid sequence encoding a therapeutic factor to promote apoptosis of endothelial cells associated with neovascularization, such that the nucleic acid is expressed thereby producing the therapeutic factor to treat ocular neovascularization prophylactically or therapeutically.
US7622469 2,4-diamino-1,3,5-triazine derivatives The present invention relates to an antibacterial agent, which comprises, as an active ingredient, a compound represented by the following general formula (1): or a pharmaceutically acceptable salt thereof.
US20090081172 Nucleic acid encoding a receptor other than an immunoglobulin, wherein the receptor binds to a MUC 1 tumor antigen independently of a major histocompatibility complex (MHC); activating a signaling pathway and/or killing a cancer cell using a receptor that is similar to or is a T cell receptor The invention provides an isolated nucleic acid encoding a receptor, other than an immunoglobulin, wherein the receptor binds to a MUC1 tumor antigen independently of an major histocompatibility complex (MHC). The invention provides a method of activating a signaling pathway and/or killing a cancer cell using a receptor that is similar to or is a T cell receptor
US20080069884 Administered intraarticular into synovial fluid; water soluble The present invention concerns amide derivatives of hyaluronic acid (HA) and biomaterials made of amide derivatives of hyaluronic acid (HA), particularly the hexadecylamide of HA, administered by the intraarticular route as a partial/total substitute for synovial fluid to treat joints affected by o steoarthrosis (OA) as well as cases of joint inflammation and/or trauma that cause damage to the cartilage and/or synovia (associated with pain). Lastly, we describe and claim their use in the treatment of joints where the entire structure shows signs of wear due to physiological aging.
WO2007088450A2 Chromane antagonist of the h-3 receptor This invention is directed to a compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula (I), a process of preparation of a compound of formula (I), a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above.
WO2010127439A1 Ammo acid derivatives for the treatment of neuropathic pain The invention relates to compounds that are amino acid derivatives, to compositions comprising the same and uses thereof for the prevention or treatment of pain, e.g. neuropathic pain, while having neutral or beneficial effect on metabolic parameters. (Formula)
EP1423378B1 Aminopyrrole compounds as antiinflammatory agents The present invention provides an aminopyrrole compound of the formula: (I) a prodrug, individual isomer, a mixture of isomers or a pharmaceutically acceptable salt thereof and methods of preparing these compounds and their use in the treatment of diseases, especially inflammatory diseases.
US20080096856 Antibiotic Compound Fermentation of a nutrient medium with a Nocardia spp. yields a novel broad spectrum antibiotic compound of structural formula (I) or a pharmaceutically acceptable salt, ester, enantiomer, diasteriomer or mixture.
US20080107609 Administering mometasone furoate and lactose particles from a multidose dry powder inhaler in daily doses of 800 mu g where at least about 250 mu g of the particles have sizes equal to or less than about 6.5 mu m. The invention relates to treating chronic obstructive pulmonary disease, involving the administration by inhalation of mometasone furoate particles in daily doses where at least about 250 μg of the inhaled particles have sizes equal to or less than 6.5 μm.
US20090221489 Water-Soluable Films Comprising Low-Viscosity Alginates A film comprising as a film-forming agent an alginate salt of monovalent cation or a mixture of alginate salts containing at least one alginate salt of monovalent cation, the film-forming agent being such that a 10% aqueous solution thereof at a temperature of 20° C. has a viscosity of 100-1000 mPas, as measured at a shear rate of 20 rpm by use of a Brookfield viscometer with a spindle No. 2. A method of preparing the film. The film is useful for delivery of active ingredients to a mammal.
WO2010092260A2 Pharmaceutical compositions of 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta (c)chromen-3-yl sulfamate The present invention relates to a solid pharmaceutical composition including the active principle 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate. The present invention also relates to polymorphs of the 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate compound.
US20060034824 Pharmaceutical composition comprising carriers for products The present patent application refers to a new product composition comprising: BROMELINE . . . more than 0.01%.
US20090137533 Convenience Kit for Eyelid Treatment The present invention offers an eyelid treatment kit used for convenient combination therapy for improving overall eyelid hygiene while also providing for adjunctive eyelid therapy. The eyelid treatment kit comprises low dose doxycycline hyclate tablets, a non-irritating eyelid cleansing composition, an anti-bacterial eyelid preparation and at least one pair of moist heat goggles and/or one pair of moisture chamber goggles. The eyelid treatment kit further comprises instruction sheets containing dosage and administration information on the doxycycline hyclate coupled with information on improving eyelid hygiene. The various embodiments of the eyelid treatment kit of the invention facilitate treatment of dry eyes due to infected eyelids, and proper cleansing of the eyelids to prevent recurring infections.
US20100303932 Method for Attenuating the Effects of Botulinum Toxin The present invention is a method for attenuating the effects of botulinum toxin poisoning using capsaicin and/or a capsaicin analog.
CN101012225A 3-Cyanoquinoline derivative, preparation method and medical use thereof The invention discloses a making method of compound I and drug composition and application to treat tumour, which is 3-cyano quinoline derivant (I) as dual-inhibitor protein kinase of tyrosine and nitric oxide synthase, wherein G1, G2, G3, G4, X, Z and n are defined as instruction.
US8569317 Aryl-quinazoline/aryl-2amino-phenyl methanone derivatives A compound of formula (1): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
US20080317883 Methods for treating depression The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and/or Formula 2 as herein defined and shown below for the treatment of depression. The present invention is directed to a method for the treatment of depression, which includes mono-therapy and alternatively, co-therapy with at least one additional antidepressant.
CN103720711A Method for preparing amphiphilic chitosan group nano iodine disinfectant The invention relates to a method for preparing amphiphilic chitosan group nano iodine disinfectant, which comprises the following steps: carrying out a grafting copolymerization reaction for chitosan or carboxymethyl chitosan and pyrrolidone derivatives and hydrophilic monomers for preparing an amphiphilic chitosan graft copolymer or amphiphilic carboxymethyl chitosan graft copolymer; carrying out a reaction between the obtained graft copolymer and iodine in a certain solvent for preparing the amphiphilic chitosan group nano iodine disinfectant or the amphiphilic carboxymethyl chitosan group nano iodine disinfectant. Compared with the prior art, the chitosan chain is grafted with pyrrolidone derivatives and other hydrophilic monomers, thereby generating the graft copolymer with amphiphilic chitosan group, and the copolymer ensures the iodine to uniformly disperse in the chitosan chain molecules; because nano iodine has good stability, compared with the existed product, the nano iodine disinfectant can remain on skin or wound for a longer time, thereby enhancing bacteriostasis effect, reducing stimulation effect of iodine on skin or wound with more security.
CN101007052A An antitumor medicine and its preparation method The invention relates to an antitumor medicament which is prepared from the following raw materials: (1) gamboges 0.5-1.5 weight parts, (2) flavescent sophora root 5-15 weight parts, or flavescent sophora root essence 0.1-0.3 weight part, sophocarpidine 0.1-0.3 weight part. The invention also discloses the process for preparing the medicament.
CN1739675A Transdermal medicine for treating cataract Medicine liquid is prepared with wolfberry fruit, chrysanthemum, vitamin C and vitamin E and administrated through transdermal application to treat cataract.
CN103381170A Applications of Chukrasone A in preparation of anti-platelet aggregation medicines The invention relates to applications of Chukrasone A in preparation of anti-platelet aggregation medicines. The applications of Chukrasone A in preparation of anti-platelet aggregation medicines are disclosed in the invention for the first time. The molecular skeleton is novel, so that the anti-platelet aggregation activity is surprisingly strong, and it is impossible to estimate the anti-platelet aggregation activity according to the anti-platelet aggregation activities of other compounds. Chukrasone A possesses outstanding substantiality, and the applications of Chukrasone A in anti-platelet aggregation possess significant advantages.
US20100256173 Method of Treating Cognitive Impairment This invention relates to the treatment and prevention of cognitive impairment, and particularly to the treatment and prevention of cognitive impairment caused by or associated with Huntington's Disease, Lewy Body Dementia, Pick's Disease and Down's Syndrome.
US7557102 Pyrazolidine-1,2-dicarboxyldiphenylamide derivatives as coagulation factor Xa inhibitors for the treatment of thromboses Novel compounds of the formula (I), in which R, R1, R2 and R3 have the meanings indicated in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.
CN103524559A Ester derivatives of multi-substituted 4-methylamino-benzamidine as well as preparation method and application of ester derivatives The invention provides new ester derivatives with a general formula (I) shown in the specification of multi-substituted 4-methylamino-benzamidine or pharmaceutically acceptable salts, wherein A1, A2, A3 and A4 in the formula are as defined in the specification. The compounds have an anticoagulant effect and can be used for preparing medicaments for preventing and treating thromboembolic diseases.
WO2010124525A1 Self micro-emulsifying oral pharmaceutical composition of hydrophilic drug and preparation method thereof A self micro-emulsifying oral pharmaceutical composition of hydrophilic drug or its pharmaceutical acceptable salt and the preparation method thereof are disclosed. The composition comprises hydrophilic drug such as bendamustine or gemcitabine, solvent, surfactant and hydrophilic carrier, and has good bioavailability and stability. Said hydrophilic carrier is compatible with drug solution and surfactant.
CA2382885C Rhodamine derivatives for photodynamic diagnosis and treatment The present invention relates to the use of the photoactivable derivatives for the photodynamic treatment for the selective destruction and/or inactivation of immunologically reactive cells without affecting the normal cells and without causing systemic toxicity for the patient, wherein appropriate intracellular levels of said derivatives are achieved and irradiation of a suitable wavelength and intensity is applied.
EP0980243B1 Use of high dose retinoids for the treatment of photodamaged skin Various skin disorders, excluding acne are treated by topical application to the skin of a retinoid-composition including a retinoid in a dermatologically acceptable vehicle at such a concentration and applied in such a way as to induce desquamation of the skin to ameliorate the disorder. Preferably, the compositions contain greater than 0.1 weight percent tretinoin, and more preferably at least 0.2 weight percent tretinoin. The vehicle is preferably a solvent for the retinoid such as an alcohol/glycol or hydroalcoholic vehicle, but it is also possible to apply the retinoid in a non-solvent vehicle such as emulsifying or suspending the retinoid in a cream, dressing, gel, ointment or liquid polymer, with or without penetration enhancers. The treatment achieves rapid amelioration of skin disorders such as photodamaged skin, hyperpigmentation, rosacea, premalignant cancers including actinic keratoses, wrinkles, superficial scarring, epidermal atrophy and atypia, and keratosis pilaris, by daily or every other day application for about one to two months. Thereafter, the high strength applications may be tapered off, and the treated skin maintained with more conventional lower concentration compositions.
US7576095 2-(p-Alkoxy- or p-fluoroalkylsulonyloxyphenyl)-1-phenyl-5-cyclohexyl- or 5-(1-piperdinyl)-4,5-dihydropyrrolo[3,2-c]pyridin-4-ones; treatment of obesity, psychiatric and neurological disorders The present invention relates to 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula IA and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
CN101165037A Beta-elemene monosubstituted ether derivatives, synthesis method and use thereof The present invention discloses monosubstituted beta-elemene ether derivative as shown and its pharmaceutically acceptable salt. The present invention also discloses the synthesis process and application in preparing anticancer medicine of the monosubstituted beta-elemene ether derivative. The monosubstituted beta-elemene ether derivative of the present invention has high water solubility, high anticancer activity, no toxicity, high medicine effect and high bioavailability.
EP1163227B1 Bicyclic heterocycles, pharmaceutical compositions containing these compounds, and processes for preparing them The present invention relates to bicyclic heterocyclic compounds of general formula (I), wherein Ra to Rd, A to D and X are defined as in claims 1 to 8, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in treating diseases, particularly tumour diseases, diseases of the lung and airways and the preparation thereof.
US8258122 3-([1,2,4]triazolo[4,3-a]pyridin-7-yl)benzamide derivatives New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed herein, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.
CN101671248A Long effective curcumin derivative and preparation method thereof The invention relates to a long effective curcumin derivative and a preparation method thereof. The long effective curcumin derivative has a structural formula, wherein R1 and R2 are hydrogen or methoxyl group; R3 and R4 are respectively and independently selected from C1 to C5 alkyl groups. The slow release effect of the long effective curcumin derivative is better than the release effect of a pure curcumin substance so that the utilization degree of the curcumin in the body can be greatly improved and the drug activity of the curcumin can be also improved, therefore, the long effective curcumin derivative has higher medical value.
CN102000104A Use of triphosadenine and derivative thereof in preparation of antidepressant and/or antianxietic medicaments The invention provides the use of triphosadenine and derivative thereof in the preparation of antidepressant and/or antianxietic medicaments. The prepared medicaments are quick in effectiveness and good in effect and have fewer side effects and long lasting action.
EP2086959A1 Substituted 2-imidazoles as modulators of the trace amine associated receptors The present invention relates to a compound of formula (I) wherein R1 is hydrogen or lower alkyl; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen or lower alkyl substituted by halogen; R is hydrogen or lower alkyl and in case when n is 2, R may be the same or not; X is -CH2-, -CH- or -O-; Y is -CH2-, -CH- or a bond; when X is -O-, Y may not be a bond; Z is -CH2- or -CH-; m is 0, 1 or 2; when m is 2, R2 may be the same or not; n is 0, 1 or 2; when n is 2, R3 may be the same or not; and to pharmaceutically acceptable acid addition salts. It has been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
US20100311673 Sulfanyl-tetrahydropyran-based compounds and methods of their use Sulfanyl-tetrahydropyran-based compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment of diseases and disorders such as diabetes and obesity are disclosed.
US20080234334 1,4 diamino bicyclic retigabine analogues as potassium channel modulators This invention is directed to compounds of formula I, where G is —O—, —S—, —C(g1)(g2)-, or —NH—, and n=1, 2, or 3. Such compounds modulate potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders which are affected by modulation of potassium ion channels. One such condition is seizure disorders.
CN103040837A Ophthalmologic intraocular pressure reduction drug for external use The invention discloses an ophthalmologic intraocular pressure reduction drug for external use. The drug takes timolol maleate as an active pharmaceutical ingredient; and the drug further comprises potassium sorbate, and the potassium sorbate is added according to the ratio that timolol maleate:potassium sorbate equals to 1:(0.1-5.0). The drug also takes tanshinone IIA as the active pharmaceutical ingredient, and the tanshinone IIA is added according to the ratio that timolol maleate:tanshinone IIA equals to 1:(0.1-5.0). The potassium sorbate-containing timolol maleate eye drops have a lasting medicinal effect, and the frequency for dropping the eye drops can be reduced.
WO2013164204A1 Tritoqualine for use in the treatment of cystic fibrosis This invention relates to tritoqualine for use in the treatment of cystic fibrosis or any one of its complications. The invention also relates to the method for the treatment of cystic fibrosis or any one of its complications by administering tritoqualine. The invention can be used to improve the condition of individuals with cystic fibrosis.
CN102964257A Ambroxol hydrochloride compound and medicine composition thereof The invention discloses an ambroxol hydrochloride crystal and a medicine composition prepared by the ambroxol hydrochloride crystal. The ambroxol hydrochloride crystal shows specific diffractive peaks in parts of 6.9 degrees, 7.2 degrees, 12.8 degrees, 15.6 degrees, 17.5 degrees, 20 degrees, 21 degrees, 22 degrees and 24 degrees in an X-ray powder diffraction pattern which is shown in form of 2 Theta +/-0.2 degrees. The prepared ambroxol hydrochloride crystal is high in yield and liquidity; and the amount of lubricant in original prescription is halved, so that the weight and uniformity of tablets can meet the specification.
WO2013136346A3 Taste masking pharmaceutical orally dissolving strips of lornoxicam A taste masking pharmaceutical orally dissolving strip of lornoxicam and the preparation process thereof. The orally dissolving strip comprises lornoxicam or pharmaceutically acceptable salts thereof as an active ingredient, taste masking agent, surfactant, and at least one pharmaceutically acceptable excipient.
US20070042439 Porphyrin compound containing biotinyl group and use thereof The present invention provides a porphyrin compound containing a biotinyl group represented by Formula (I): Por-A-Bi wherein Por represents a porphyrin residue optionally forming a metal complex; Bi represents an optionally substituted biotinyl group; and A represents a C1-C20 hydrocarbyl group, or a heterohydrocarbyl group having 1-5 heteroatoms selected from a group consisting of oxygen, sulfur, and nitrogen, and having 1-20 atoms in total; a method for purifying hemoprotein which use the porphyrin compound; a hemoprotein labeling reagent; a diagnostic agent for hemoprotein associated diseases which use the porphyrin compound; and a therapeutic agent for photodynamic therapy.
EP1646644A2 Posh interacting proteins and related methods The application provides novel complexes of POSH polypeptides and POSH-associated proteins. The application also provides methods and compositions for treating POSH-associated diseases such as viral disorders, cancer, and neurological disorders.
US20070244063 Inducing angiogenesis comprising contacting endothelial cells expressing Bv8 receptor with a polypeptide comprising the amino acid sequence of SEQ ID NO:2; using Bv8 polypeptides to induce endothelial cell proliferation and to enhance endothelial cell survival; screening for Bv8 modulators The present invention provides methods of using Bv8 polypeptides to induce endothelial cell proliferation and to enhance endothelial cell survival. Also provided herein are methods of screening for modulators of Bv8 activity. Furthermore, methods of treatment using Bv8 polypeptides are provided.
CN102908345A Drug composition suitable for transdermal drug delivery and containing granisetron as well as preparation and application of same The invention relates to a drug composition containing granisetron. The drug composition comprises a sodium polyacrylate pressure-sensitive adhesive (A), a polyacrylic resin (B), a penetration enhancer (C) and granisetron (D), wherein the sodium polyacrylate pressure-sensitive adhesive (A) is a (methyl) acrylate copolymer containing (methyl) acrylamide or N, N-substituted monomer thereof; the polyacrylic resin (B) is an Eudragit polyacrylic resin; and the penetration enhancer (C) is selected from isopropyl myristate, azone, glyceryl triacetate and 1, 2-propylene glycol as well a a mixture thereof. A granisetron transdermal patch containing the drug composition obtains satisfactory technical effects on mechanical property, skin irritation and the like; more importantly, the transdermal patch obtains considerable transdermal flux when the excellent performances are guaranteed.
CN103127086A Application of Eryngiolide A in medicines curing or preventing dental ulcer The invention relates to application of Eryngiolide A in preparation of medicines curing and preventing dental ulcer. Use of the Eryngiolide A in preparation of medicines curing or preventing dental ulcer is made public for the first time, due to the fact that the skeleton type is completely novel, and the Eryngiolide A has an unexpectedly high activity of curing the dental ulcer, probability of other compounds giving any revelation for the Eryngiolide A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in curing dental ulcer.
US20100305176 (s,r.)-3-phenyl-4,5 dihydro-5-isoxazole acetic acid-nitric oxide and use thereof as anti-cancer and antiviral agent The present invention relates to an isoxazole derivative, the compound of formula (I) herein after referred to as GIT27-NO, which is the NO-donating structurally modified form of (S,R)-3-phenyl-4,5-dihydro-5-isoxazole acetic acid, herein after referred to as VGX-1027. Treatment of three tumor cell lines, rat astrocytoma C6, mouse fibrosarcoma L929, and mouse melanoma B16 cells with GIT27-NO resulted in a significant reduction of cell respiration and of number of viable cells, while VGX-1027 was completely ineffective. Hemoglobin, which act as NO-scavenger, restored cell viability, thus indicating the NO-mediated tumoricidal effect of compound (I). GIT27-NO triggered apoptotic cell death in L929 cell cultures, while autophagic cell death is mainly responsible for the diminished viability of C6 and B16 cells. Moreover, GIT27-NO induced the production of reactive oxygen species which can be neutralized by antioxidant N-acetyl cysteine (NAC), indicating that reactive oxygen species (ROS) are at least partly involved in the reduction of cell viability. The anti-tumor activity of GIT27-NO is mediated through activation of MAP kinases (ERK1/2, p38 and JNK) in cell-specific manner. The role of MAP kinases was further confirmed by specific inhibitors of these molecules, PD98059, SB202190, and SP600125. Finally, in vivo treatment with GIT27-NO significantly reduced tumor growth in syngeneic C57BL/6 mice implanted with B16 melanoma.
CN102688477A Medicinal composition for treating respiratory diseases of livestock The invention provides a medicinal composition for treating respiratory diseases of livestock, which comprises the following active components in percentage by mass: 5 to 8 percent of tilmicosin, 3 to 5 percent of cefquinome, 20 to 30 percent of astragalus polysaccharides, 5 to 8 percent of kameiding, 3 to 5 percent of muramyl dipeptide, 5 to 8 percent of ribavirin, 6 to 10 percent of oligosaccharide, and 45 to 55 percent of anhydrous sugar. The drugs are mixed, and have the functions of clearing heat and removing toxicity, relieving cough and asthma, have unique curative effect for treating respiratory diseases of livestock, have no drug resistance, and have quick response, good curative effect and short course of treatment.
US6989445 Substituted [1,4]oxazino[2,3-g]indazoles for the treatment of glaucoma Substituted [1,4]oxazino[2,3-g]indazols for lowering intraocular pressure and treating glaucoma are disclosed.
US20120245182 Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1--1-methyl-urea and salts thereof The present technology provides novel anhydrous and hydrated crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, amorphous and anhydrous crystalline polymorphs of its monophosphoric acid salt, and the hydrochloride salt, including its dihydrate. The present technology further provides methods for preparing the various forms, compositions containing them, and methods of treatment employing them.
CN101991542A Lansoprazole enteric dry suspension and preparation method thereof The invention relates to lansoprazole enteric dry suspension and a preparation method thereof. The lansoprazole enteric dry suspension comprises the following components in percentage by weight: 15 percent-50 percent of lansoprazole pellets or particles, 1 percent-10 percent of suspending agents and 50 percent-85 percent of flavoring agents. The prepared lansoprazole enteric dry suspension has the advantages of stable quality, quick response, good suspension effect and high biological utilization degree, and is convenient for old people, children and patients suffered from dysphagia.
CN101332190A Sugar-free type citrulline effervescence tablet and preparation method thereof The present invention relates to a sugarless citrulline effervescent tablet and a preparation method thereof. The raw material components of the sugarless citrulline effervescent tablet include 5 to 50 parts of xylitol, 0.5 to 90 parts of citrulline, 2 to 5 parts of low substituted carboxyprpyl fibrin, 5 to 20 parts of sodium bicarbonate, 0.1 to 0.6 part of essence and 1 to 4 parts of magnesium stearate. The raw material components are subject to the steps of mixing, preparing for being soft material, pelletizing, finishing, tabletting, and the like, to obtain a product of the present invention. The product of the present invention is sugarless, is convenient for carrying and eating, has clean and fresh taste and can provided ordinary people with nutrition and also meet the requirement of sports people; at the same time, the sugarless citrulline effervescent tablet can also satisfy the long term treatment requirement of male ED patient according to different citrulline contents and dosages; the sugarless citrulline effervescent tablet has the advantages of simple preparation method and relative low cost.
CN103172555A Indole alkaloid compound separated from rhizoma cimicifugae as well as preparation method and application thereof The invention provides an indole alkaloid compound separated from rhizoma cimicifugae as well as a preparation method and an application thereof. The compound provided by the invention is a novel indole alkaloid compound which is separated from rhizoma cimicifugae. The invention further provides a pharmaceutical composition which contains the compound or pharmaceutically acceptable salts thereof, and an application of the compound in preparation of antitumor medicines.
CN101070274A Diphenylethene compound with anti-tumor activity and preparing method This invention belongs to plant medicinal ingredient and tumour-resisting toluyleneonium compounds region, refer a antineoplastic activity toluylene compounds and preparation method. The structural formula as chart described: the R and R' respectively is any one of - H, - CH3, - CH2CH3, - CH2CH=C ( CH3) 2, - OH, - OCH3, - NH2, O=CCH=CH ( CH3)2. Test show that, this invention has inhibitory action to manifold tumor cell growth and proliferation.
CN102911157A (E)-3-[2-bromo-5-(3-substituted propoxy)]phenyl-N-{4-methyl-3-[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl acrylamide compound The invention belongs to the technical field of medicines, and relates to a (E)-3-[2-bromo-5-(3-substituted propoxy)]phenyl-N-{4-methyl-3-[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl acrylamide compound and pharmaceutically acceptable salts thereof. The compound has the structural formula represented below, wherein R is piperazinyl, 3-methylpiperazinyl, 4-methylpiperazinyl, 3,5-dimethylpiperazinyl, piperidinyl, tetrahydropyrrole, morpholinyl, dimethylamino, or diethylamino; and a double-bond is E type. The invention also relates to preparation methods of the compound and the pharmaceutically acceptable salts thereof, and compositions containing the compound. The (E)-3-[2-bromo-5-(3-substituted propoxy)]phenyl-N-{4-methyl-3-[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl acrylamide compound and the pharmaceutically acceptable salts thereof have good anti-cancer activity. The preparation methods are simple and feasible, and are easy to operate.
CA2326529C 2-(3,5-bis-trifluoromethyl-phenyl)-n-methyl-n-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide The invention relates to the compound of the formula (see formula I) which is 2-(3,5-bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o- tolyl- pyridin-3-yl)-isobutyramide. It has been found that this compound has a high affinity to the NK- 1 receptor and it is therefore useful in the treatment of diseases, which relate to this receptor.
DE102005003865A1 Oral composition, useful e.g. to enhance brain function, comprises phosphatidylserine and a flavor compound or its precursor Phosphatidylserine-based oral composition (I) for enhancing brain function comprises phosphatidylserine (PS) and at least a flavor compound or its precursor as active components. - ACTIVITY : Cerebroprotective; Nootropic. The ability of (I) to improve the memory power and cognitive ability was tested in human. The result showed that (I) significantly improved the memory power and the cognitive ability in two months. - MECHANISM OF ACTION : None given.
US7005408 Anhydrous warming, non- toxic and nonirritating lubricating compositions containing polyhydric alcohols and an insulating agent. The invention also relates to methods of using such compositions for lubrication, administration of active This invention relates to substantially anhydrous warming, non-toxic and nonirritating lubricating compositions containing polyhydric alcohols and an insulating agent. The invention also relates to methods of using such compositions for lubrication, administration of active ingredients and for preventing or treating dysmenorrhea.
CN101708334A Medicament for treating animal dermatosis The invention discloses a medicament for treating animal dermatosis. The medicament is prepared by a method comprising the following steps: firstly, scraping a secretion or a pus from an animal wound skin, inoculating the secretion or the pus into a nutrient agar medium, culturing the nutrient agar medium in an incubator for 48h, taking out a grown bacterium pure culture on the third day to perform a medicament sensitive test, and selecting a high-sensitivity antibiotic for later use; secondly, putting 200g of sublimed sulfur powder which passes through a 100-mesh sieve in the center of an ointment slab, uniformly grinding 600g of medical vaseline and the sublimed sulfur powder to obtain a sulfur ointment; and finally, taking the prepared sulfur ointment and the high-sensitivity antibiotic, and uniformly stirring the high-sensitivity antibiotic and the sulfur ointment according to the rule that 1.5 million IU of the high-sensitivity antibiotic is added into every 50g of sulfur ointment to obtain a finished product. The method for preparing the medicament is simple and feasible; and the prepared medicament has very good curative effect on intractable dermatosis of animals and is in favor of increasing the survival rate of livestock.
DE102005005395A1 New thiazolidinone compounds are polo-like kinase inhibitors, useful for treating e.g. cancer, autoimmune diseases, cardiovascular diseases, infectious diseases, nephrological diseases and viral diseases Thiazolidinone compounds (I) and their salts, solvates, hydrates, stereoisomers, diastereomers and enantiomers are new. Thiazolidinone compounds of formula (I) and their salts, solvates, hydrates, stereoisomers, diastereomers, and enantiomers are new. Q : (hetero)aryl; A, B1>1-6C alkyl or 1-6-C alkoxy (both optionally substituted by halo, -OH, 2-9C heterocycloalkyl, -NR3>R4> or -CO(NR3>)-M) (where the heterocycloalkyl contains N, O or S and optionally: interrupted by -(CO)-, -SO2- or double bond in the ring; and the ring is optionally substituted by -CN, halo, halo substituted 1-6C alkyl, 3-6C cycloalkyl, 1-6C hydroxyalkyl, -COR2> or -NR3>R4>), H, halo, -OH, -NH2, -NO2, NR3>R4>, -NR3>(CO)-L, -NR3>(CO)-NR3>-L, -COR2>, -CO(NR3>)-M, -NR3>(CS)NR3>R4>, -NR3>SO2-L, -SO2-NR3>R4> or -SO2(NR3>)-M; L : 1-6C alkyl or heteroaryl (both optionally substituted by -OH, 1-6C hydroxyalkoxy, 1-6C alkoxyalkoxy, 2-6C heterocycloalkyl or -NR3>R4>, where the heterocycloalkyl contains N, O or S and optionally interrupted by -(CO)-, -SO2- or double bond in the ring; and the ring is optionally substituted by -CN, halo, halo substituted 1-6C alkyl, 3-6C cycloalkyl, 1-6C hydroxyalkyl, -COR2> or -NR3>R4>); M : 1-6C alkyl (optionally substituted by -NR3>R4> or 2-6C heterocycloalkyl), where the heterocycloalkyl contains N, O or S and optionally interrupted by -(CO)-, -SO2- or double bond in the ring; and the ring is optionally substituted by -CN, halo, halo substituted 1-6C alkyl, 3-6C cycloalkyl, 1-6C hydroxyalkyl, -COR2> or -NR3>R4>; either W1>heteroaryl or 2-9C heterocycloalkyl, where the heterocycloalkyl contains N, O or S and optionally interrupted by -(CO)-, -SO2- or double bonds in the ring; and X, Y1>1-6C alkyl, aryl (both optionally substituted by halo, -OH, 1-6C alkoxy, 1-6C alkylthio or aryl), -COOR5>, -CONR3>R4> or H; or W1>+X+Y1>3-6C cycloalkyl ring or 2-6C heterocycloalkyl ring, where the heterocycloalkyl contains N, O or S and optionally interrupted by -(CO)-, -SO2- or double bonds in the ring; and the ring is optionally substituted by 1-6C alkyl, 3-6C cycloalkyl, 1-6C hydroxyalkyl or -NR3>R1>; R1>1-4C alkyl, 3C-cycloalkyl, allyl or propargyl (all optionally substituted by -CN or halo); R2>-OH, 1-6C alkyl, 1-6C alkoxy or -NR3>R4>; either R3>, R4>1-6C alkyl, 1-6C alkoxy, CO-(1-6C)-alkyl, aryl (all optionally substituted by halo, -OH, 2-6C heterocycloalkyl, 1-6C hydroxyalkoxy or -NR3>R4>) or H, where the heterocycloalkyl contains N, O or S and optionally interrupted by -(CO)-, -SO2- or double bond in the ring; and 2-6C heterocycloalkyl ring substituted by -CN, halo, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C alkoxy, 3-6C cycloalkyl, -NR3>R4> or -CO-NR3>R4>; or R3>R4>2-6C heterocycloalkyl ring, where the heterocycloalkyl contains N, O or S and optionally interrupted by -(CO)-, -SO2- or double bonds in the ring; and the ring optionally substituted by halo, 1-6C alkyl, 3-6C cycloalkyl, 1-6C hydroxyalkyl, 1-6C alkoxyalkyl, -CN, -OH or -NR3>R4>; and R5>1-6C alkyl (optionally substituted by halo, -OH, 2-6C heterocycloalkyl, 1-6C hydroxyalkoxy or -NR3>R4>), where the heterocycloalkyl contains N, O or S and optionally interrupted by -(CO)-, -SO2- or double bonds in the ring; and the ring optionally substituted by 1-6C alkyl, 3-6C cycloalkyl, 1-6C hydroxyalkyl, 1-6C alkoxyalkyl, -CN, -OH or -NR3>R4>. An independent claim is also included for an intermediate substituted heterocyclic compound of formula (II). Rx>1-3C alkyl. [Image] [Image] - ACTIVITY : Cytostatic; Immunosuppressive; Endocrine-Gen.; Cardiovascular-Gen.; Antimicrobial; Neuroprotective. - MECHANISM OF ACTION : Polo-like kinase inhibitor.
CN103610669A Bis-(p-alkoxy benzene acrylketone) like glutathione-S-transferase potential inhibitor The invention discloses a bis-(p-alkoxy benzene acrylketone) like glutathione-S-transferase potential inhibitor. Structure and living features of the potential inhibitor are as follows: two p-alkoxy benzene acrylketone units are linked to two amino groups, alcoholic hydroxyl groups and carboxyl groups or one amino group and one alcoholic hydroxyl group which are spaced by less than 8 single bonds through amide and/or ester bond, wherein compounds obtained are substrate and inhibitor of glutathione-S-transferase, namely GST; the GST catalyzes carbon-carbon bond and reduced glutathione, namely GSH, of alpha, beta-unsaturated ketone of each p-alkoxy benzene acrylketone unit in the compounds and generates a compound, namely product, through Michael addition. The product shows a stronger inhibiting efficacy on the GST, so that the compound is a GST potential inhibitor; the product has a stronger inhibiting efficacy on human GST isozyme mu in comparison with human GST isozyme alpha and pi; and the compounds can enter into cells, and can enhance inhibiting effect of cis-platinum on drug-resistant carcinoma cell growth.
CN103610658A Immunomodulator slow-release preparation and preparation method thereof The invention discloses an immunomodulator slow-release preparation and a preparation method thereof. A lenalidomide slow-release tablet is composed of a slow-release layer and an optional quick-release layer, wherein the slow-release layer contains active ingredients of lenalidomide and a slow-release framework material simultaneously; the quick-release layer does not contain the slow-release framework material. The lenalidomide slow-release tablet disclosed by the invention is capable of slowly and uniformly releasing medicines by virtue of the slow-release framework material, so as to reduce the release speed, delay the time to peak, prolong the action time of lenalidomide, and provide a uniform and constant blood concentration. Moreover, The lenalidomide slow-release tablet disclosed by the invention is simple in prescription and excellent in quality stability; the preparation process is simple to operate, free from special treatment and production equipment, low in production cost, and beneficial to batch-enlarged industrial production for the product; the preparation method is high in yield, the granulation and crushing procedures are simple and practicable to operate, the intermediate material is good in stability, flowability, compressibility and content uniformity, and completely meets the requirements of tabletting, and the surface of the prepared tablet is smooth and beautiful.
WO2008128995A1 4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists The present invention relates to (1-benzyl-piperidin-4-yl) - (4-alkoxy-pyridazin-3-yl) - amines of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
US20100041747 Use of certain chemical compounds for the inhibition of the peptidyl-prolyl cis/trans isomerase activity of cyclophilins The present invention relates to the use of certain spiro, ketone and carboxylic acid compounds for the inhibition of the peptidyl-prolyl cis/trans isomerase activity of cyclophilins and the use of these compounds for the production of a cosmetic or pharmaceutical composition for the promotion of hair growth or for the treatment or prevention of inflammatory autoimmune diseases, of diseases caused by fungi, of bacterial infections, of viral infections, of diseases caused by parasites, protozoa or worms, of cancer, of diseases of cells, of fibrosing diseases, and of non-neoplastic changes and diseases which are attributable to prions and changes in the structure and function of cellular proteins and cells.
US20070254958 by preventing the formation of insoluble beta-amyloid and arresting the production of beta-amyloid; e.g. 3-{2-[(5-aminopentyl)amino]-2-oxoethoxy}-5-({[(1R)-1-(4-fluorophenyl)ethyl]amino}carbonyl)phenyl phenylmethanesulfonate The present invention is directed to phenyl carboxamide compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
WO2009093209A3 2-ALKYLAMINO-3-ARYLSULFONYL-CYCLOALCANO [e OR d] PYRAZOLO [1,5-A]PYRIMIDINES / ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND THE USE THEREOF The invention relates to antagonists of serotonin 5-HT6 receptors, substituted 2-alkylamino-3-arylsulfonyl-cycloalcano [e or d] pyrazolo [1,5-a]pyrimidines, medicinal principles and pharmaceutical compositions which contain the medicinal principles in the form of the above-mentioned compounds, to novel medicinal agents and to a method for treating and preventing the development of CNS diseases. The invention discloses 2-alkylamino-3-arylsulfonyl-cycloalcano [e or d] pyrazolo [1,5-a]pyrimidines of general formula (1) and 2-alkylamino-3-arylsulfonyl-cycloalcano[e or d]pyrazolo [1,5-a]pyrimidines of general formula (2), wherein R1 is a hydrogen atom or C1-C3 alkyl; R2 is C1-C3 alkyl; R3 is an hydrogen atom, one or two optionally the same halogen atoms, C1-C3 alkyl and optionally alkyl-substituted hydroxyl; and n is an integer 1, 2 or 3.
US20050118253 comprising a nucleic acid that is fully encapsulated within a lipid; for treating a neoplasia in a mammal The present invention relates to methods and compositions for treating a neoplasia in a mammal.
CN1846690A Emulsion medicine injection of propofol and its prepn process The present invention relates to emulsion medicine injection of propofol comprising propofol, metal ion chelating agent and cysteine. The present invention solves well the problem of the oxidation of phenol hydroxyl group in effective component propofol to produce degradation product and can ensure safety of clinical administration.
CN101879170B Anti-tumor application of malonyl astragaloside I and aglycon thereof The invention relates to the field of natural medicaments, in particular to the anti-tumor application of tetracyclic triterpene type compounds of malonyl astragaloside I and cycloastragenol thereof which can be used for preparing anti-tumor medicaments and particularly preparing medicaments for treating intestinal cancer, leukemia, lung cancer or liver cancer.
EP2374814A2 Peptides that ellicit T cellular immunity The invention relates to peptides from cancer related protein products of frameshift mutated genes, said protein products eliciting T cellular immunity, for use in cancer vaccines and compositions for anticancer treatment. In particular the invention relates to protein products of frameshift mutated BAX or TGFβRII genes.
CN103120674A Application of Eryngiolide A in preparation of MAO (Monoamine Oxidottom) inhibitor The invention discloses an application of Eryngiolide A in preparation of an MAO (Monoamine Oxidottom) inhibitor. Compared with the existing monoamine oxidase inhibitor, the MAO inhibitor is greatly enhanced in inhibitory activity and selectivity on MAO-A and MAO-B. The application of the Eryngiolide A in preparation of the MAO inhibitor is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Eryngiolide A on monoamine oxidase is inconceivably high; and the Eryngiolide A has outstanding substantiality characteristic without possibility of any inspiration given by other compounds and obviously achieves the outstanding progress by being used for treating monoamine oxidase maladjustment related diseases.
CA2673803A1 Compounds and compositions as channel activating protease inhibitors The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
EP1539186A1 Combination therapy comprising a bisphosphonate and a hmg-coa reductase inhibitor A pharmaceutical composition for treatment of malignancies, in particular multiple myeloma (MM), comprises in combination a bisphosphonate, e.g. zoledronic acid or a salt or ester, and an HMG-CoA reductase inhibitor for simultaneous, sequential or separate use. Also provided is a method of treating a patient suffering from a malignant disease comprising administering to the patient an effective amount of a bisphosphonate and an effective amount of an HMG-CoA reductase inhibitor.
US6887469 Anti-idiotypic antibodies of vascular endothelial growth factor and use thereof as drugs An anti-idiotypic vascular endothelial growth factor antibody, an Fab fragment, and pharmaceutical compositions thereof, being ligands of the human KDR receptor or of the murine flk-1 receptor and not a ligand of flt are provided.
CN103301143A Application of polyflavanostilbebe A in preparation of medicament for treating or preventing dengue virus infection The invention discloses the application of polyflavanostilbebe A in preparation of a medicament for treating or preventing dengue virus infection. The polyflavanostilbebe A can effectively inhibit the proliferation of dengue viruses, has low toxicity to cells, and can be further developed to obtain medicaments for treating diseases caused by the dengue virus infection, so that the polyflavanostilbebe A has a wide application prospect. The application of the polyflavanostilbebe A in the preparation of the medicament for treating or preventing the dengue virus infection is disclosed for the first time; because a skeleton type belongs to a new skeleton type, the inhibitory activity of the polyflavanostilbebe A on the dengue virus is unexpectedly high and is impossibly revealed by any other compounds, and the polyflavanostilbebe A has prominent substantive characteristics and obviously has significant progress in prevention and treatment of the dengue virus infection.
US7226926 8-fluoroimidazo 1,2-a pyridine derivatives as ligands for GABA receptors A class of 8-fluoroimidazo[1,2-α]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
CN101347596A External-use plaster for treating beriberi The invention relates to an external plaster for treating dermatophytosis and is characterized in that the plaster is prepared by the raw materials according to the following weight ratio: 10-20 parts of rhizoma zedoariae, 5-15 parts of herba schizonepetae, 10-30 parts rhizoma coptidis, 5-40 parts of baikal skullcap root, 8-15 parts of phellodendron, 20-60 parts of tarragon, 10-15 parts of borneol, 15-30 parts of plaster and 20-30 parts of myrrh. By being applied with the medicines together, the external plaster has the functions of internal and external application, effectively curing dermatophytosis, achieving the effects of removing heat and dampness, detoxification and relieving itching as well as invigorating the circulation of blood and generating myocomma. The dermatophytosis is not easy to recur after being cured.
US20120095019 Methods and formulations of treating thrombosis with betrixaban and a p-glycoprotein inhibitor This invention is directed to methods of inhibiting coagulation or treating thrombosis using a factor Xa inhibitor and a P-glycoprotein (Pgp) inhibitor. The invention is also directed to formulations used in the methods.
EP2055705A1 Compound having cyclic group bound thereto through spiro binding and use thereof A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy.
US20060035895 Isoxazoline derivatives useful as antimicrobials Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an N-linked 5-membered, fully or partially unsaturated heterocyclic ring, or HET is an N-linked 6-membered di-hydro-heteroaryl ring; Q is, for example, Q1 or Q2: wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example a group of the formula (TC7) wherein Rc is, for example, hydrogen, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1-10C)alkyl or R14C(O)O(1-6C)alkyl wherein R14 is optionally substituted (1-10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
WO2014001802A1 2-aminopyrazine derivatives as csf-1 r kinase inhibitors The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein:ring A, R1, R2, n, X, V, W, Z, ring B, [Linker] and R areas defined herein. The compounds are useful as inhibitorsof CSF-1R kinase. The compounds can thus be used in medicine.
WO2008136838A1 Novel amide derivatives of cddo and methods of use thereof The invention concerns novel synthetic triterpenoids, such as CDDO-EA and CDDO-TFEA, and their use for the treatment and prevention of diseases, such as MS.
CN101336915A Medicine combination with antitumor activity The invention relates to a pharmaceutical composition, particularly to a pharmaceutical composition with antitumor activity. The pharmaceutical composition with antitumor activity comprises 5,6-dimethylxanthenone-4-acetic acid (DMXAA) or an pharmaceutically acceptable salt or ester thereof and one drug component selected from glycopeptide antibiotics, actinomycins, mitomycins, glucoside antibiotics, Colchicum alkaloid, elemenes, aromatic enzyme inhibitors, LH-RH receptor antagonists, animal antitumor drugs and somatostatin analogues. The synergic composition has better antitumor activity. More specifically, the invention provides an application of the composition in treating tumors.
CA2164717C Method of combatting hepatitis b virus infection A method of treating hepatitis B virus is disclosed. The method comprises administering to a subject in need of such treatment a hepatitis B combatting amount of alkyl ether phospholipids and alkyl ether phospholipid derivatives.
WO2010093425A1 Histamine h3 inverse agonists and antagonists and methods of use thereof Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
US20120009190 Identification and method for using the pre-ligand assembly domain of the il-17 receptor The invention provides isolated Pre-Ligand Assembly Domain (PLAD) polypeptides comprising an amino acid sequence of a domain (e.g., a Fibronectin Ill-like domain) of an IL-17 Receptor (IL-17R) family member, wherein the PLAD polypeptide inhibits multimerization of a receptor complex comprising an IL-17R family member. Also provided are isolated PLAD-binding polypeptides, e.g., antibodies and avimers, which specifically bind to a PLAD polypeptide described herein. Related chimeric proteins, conjugates, nucleic acids, vectors, and host cells are provided herein. Further provided are methods of treating an inflammatory or autoimmune disease, methods of inhibiting IL-17-mediated signal transduction, methods of inhibiting IL-17 ligand binding, methods of inhibiting multimerization of IL-17R complexes, and methods of inhibiting the production of at least one cytokine, chemokine, matrix metalloproteinase, or other molecule associated with IL-17 signal transduction are provided.
WO2009145831A1 Treatment of the idiopathic nephrotic syndrome spectrum diseases using basiliximab Methods for treating Idiopathic Nephrotic Syndrome Spectrum (INSS) diseases using antibodies to the IL-2 receptor (anti-IL-2r antibodies) of T cells, such as basiliximab are described. The methods may be used for treating the broad spectrum of INSS diseases in both children and adults.
WO2007041294A3 Methods for sensitizing cancer cells to inhibitors The present invention is based on the discovery that inactivation of the heat shock response in cancer cells significantly enhances their sensitivity to proteasome and Hsp90 inhibitors. The inventors have discovered novel compounds which exhibit low toxicity, inhibit the heat shock protein response and sensitize cancer cells to anti- cancer therapies. In general, the heat shock protein inhibitors of the present invention share a common structure, namely a 2H-benzo[a]quinolizine tricyclic ring. Also encompassed are methods for a high throughput screen to identify heat shock inhibitors that sensitize cancer cells to anti-cancer therapies.
EP2015647A2 Iron complex for use in the treatment and/or prevention of nutritional disorders This invention relates to certain iron complexes which comprise ferrous or ferric iron and mono-, bi-, tri- or hexadentate ligands containing a five- or six-membered aromatic or heterocyclic ring for use in the treatment and/or prevention of nutritional disorders and compositions containing such iron complexes. The iron complexes enhance the bioavailability of the iron and are particularly useful in the treatment and/or prevention of nutritional disorders, iron deficiency disorders and anaemia.
CN101830911B Thienopyridine derivatives, preparation method and application thereof The invention belongs to the technical field of drugs resisting platelet aggregation, in particular to thienopyridine derivatives with the structure of a formula I and salts thereof, wherein n is equal to 0 and 1; R1 is C1-C4 alkyl; R2 and R3 are simultaneously or respectively hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen and halogenated methyl; and R4 is C1-C4 alkyl. The invention also relates toa preparation method of the compounds, and discloses a drug composition with the compounds or salts thereof as active effective components, and application of the compounds in preparing the drugs forresisting the platelet aggregation.
US20110319476 Treatment of glial cell derived neurotrophic factor (gdnf) related diseases by inhibition of natural antisense transcript to gdnf The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Glial cell derived neurotrophic factor (GDNF), in particular, by targeting natural antisense polynucleotides of Glial cell derived neurotrophic factor (GDNF). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of GDNF.
EP2497459A1 Methods of reducing microbial contamination The present invention relates to an antimicrobial composition for use in delaying the onset of an infection or preventing an infection caused by a microbial organism in an internal cavity of a subject, wherein the antimicrobial composition comprises: an effective amount of an antimicrobial component comprising (i) one or more antimicrobial lipid antiseptics comprising one or more fatty acid esters of a polyhydric alcohol, one or more fatty ethers of a polyhydric alcohol, or alkoxylated derivatives of either or both of the ester and ether, or combinations thereof; wherein the antimicrobial composition includes the one or more antimicrobial lipids in a total amount of at least 0.25 wt-%, based on the total weight of the antimicrobial composition; and/or (ii) iodine and/or an iodophor, wherein the available iodine concentration is at least about 0.05 wt-%, based on the total weight of the antimicrobial composition; a hydrophilic component; and a surfactant component distinct from the antimicrobial component; with the proviso that when the internal cavity comprises a nasal passage, vagina, or oral cavity, the antimicrobial component does not include iodine or chlorhexidine; and wherein the antimicrobial composition is to be administered in a method comprising the steps of: contacting at least a portion of the interior surface of an opening leading to the internal cavity with an antimicrobial composition; and subsequently at least partially inserting an instrument into the opening.
WO2013174895A1 Heterocyclyl pyrimidine analogues as tyk2 inhibitors The present invention relates to compounds of formula (I), wherein R, R1, X1 to X5 have the meaning as cited in the description and the claims. Said compounds are useful as TYK2 inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds as well as their use as medicaments.
US20110053861 Compositions comprising nuclear factor-kappa b (nf-kb) sirna and methods of use The present invention provides siRNA nucleic acid molecules that inhibit NF-kappaB expression. Methods of using the nucleic acid molecules are also provided.
EP2234985B1 4-(4-cyano-2-thioaryl)dihydropyrimidinones and use thereof The present application relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for preparation thereof, to the use thereof alone or in combination for treatment and/or prevention of disorders, and to the use thereof for production of medicaments for treatment and/or prevention of disorders, especially for treatment and/or prevention of disorders of the lung and of the cardiovascular system.
US6890546 Stents, catheters, arterio-venous grafts, by-pass grafts and drug delivery ballons with surface coating containing a rapamycin derivative having a tetrazole group A medical device comprising a supporting structure having a coating on the surface thereof, the coating containing a therapeutic substance, such as, for example, a drug. Supporting structures for the medical devices that are suitable for use in this invention include, but are not limited to, coronary stents, peripheral stents, catheters, arterio-venous grafts, by-pass grafts, and drug delivery balloons used in the vasculature. Drugs that are suitable for use in this invention include, but are not limited to,
CN103127096A Application of pyrryl-substituted indole compound in curing glaucoma The invention discloses application of pyrryl-substituted indole compound in curing glaucoma. The pyrryl-substituted indole compound can cure glaucoma through small-dose multiple intraocular injection medicine administration and eye drop multiple medicine administration. Furthermore, after the pyrryl-substituted indole compound is coated by lipidosome or is prepared into high-polymer-coated nanometer medicine, micro-ball drug medicine and hydrogel medicine, glaucoma can be cured continuously after intraocular medicine injection to achieve obvious medicine effects.
CN103086861A Hydroxydecyl benzoquinone derivative and application thereof The invention relates to a hydroxydecyl benzoquinone derivative and application thereof. The invention specifically relates to a hydroxydecyl benzoquinone derivative shown as the following compound with a formula I, a pharmaceutical composition comprising the compound, a preparation method of the benzoquinone derivative as well as application of the derivatives in preparation of medicines for cerebrovascular diseases.
WO2008095821A1 Indol-2-yl-piperazin-1-yl-methanone derivatives The present invention relates to compounds of formula (I), wherein A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
US7081467 C2-disubstituted indan-1-ones and their derivatives, processes for their preparation and their use as pharmaceuticals The present invention is directed C2-disubstituted indan-1-ones of the Formula I, physiologically acceptable salts, and physiologically functional derivatives thereof, and pharmaceutical compositions comprising such compounds, salts and derivatives, which are useful for reducing weight, for the prophylaxis or treatment of obesity, and for the prophylaxis or treatment of type II diabetes in mammals. The invention is directed also to methods for reducing weight and such treatments and prophylaxis. The invention is directed also to processes for the preparation of such compounds.
WO2011110190A1 A cellobiose compound from herbal extracts having apoptotic activity The present invention refers to a compound isolated from a combination of herbal extracts of Capsicum chinense and Allium neapolitanum having apoptotic activity in cancer cells, which compound was identified as cellobiose. In particular, the present invention refers to a cellobiose compound for use in the prevention and treatment of cancer. The present invention further refers to a pharmaceutical composition comprising a cellobiose compound. The present invention also refers to a use of a cellobiose compound for inducing apoptosis in a cell or a tissue system in vitro.
US20090271217 Side effect ameliorating combination therapeutic products and systems Combination therapeutics, computer program products, and systems are described that include at least one combined prescription psychiatric medication and at least one artificial sensory experience for ameliorating at least one side effect of the psychiatric medication.
CN103751782A New application of weakly alkaline solution The invention belongs to the field of medicine and health, and relates to application of a solution with pH of 7-9. The solution is used for preparation of a sprayer for nursing mammal oral cavity, balancing oral-cavity pH value and preventing and treating oral-cavity diseases.
CN102250143A Imidazole benzamide compounds and application thereof in preparation of anti-malignant tumor medicaments The invention relates to imidazole benzamide compounds and application thereof in the preparation of anti-malignant tumor medicaments. The imidazole benzamide compounds belong to a tyrosine kinase inhibitor having high selectivity, and can inhibit the activity of KIT and PDGFR (platelet-derived growth factor receptor) kinases. Besides, the imidazole benzamide compounds can be used for the preparation of medicaments, including but not limited to medicaments for treating imatinib resistant or intolerant CML (chronic myeloid leukemia) and refractory or recurrent Ph chromosome positive acute lymphatic leukemia, medicaments for treating gastrointestinal stroma cell tumors and medicaments for treating initially-treated systemic mastocytosis.
WO2012125544A3 Necroptosis inhibitors and methods of use therefor Described herein are compositions that inhibit the production of TNFα downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNFα production or CD40 activation.
CN103520011A Application of tetrahydropalmatine and baicalin in preparing oral care products The invention discloses application of tetrahydropalmatine and baicalin in preparing oral care products, i.e., tetrahydropalmatine and baicalin are added into an oral care health-care product as active ingredients with analgesic effect in form of a compound in a process of preparing oral care products. Compared with the prior art, the oral care products provided by the invention not only are safe to use, but also have remarkable analgesic effects.
CA2621370A1 Salicylate and gentisate salts of a piperazine compound . The present invention provides salt forms of the formula below wherein R is H or OH, and compositions thereof, useful as modulators of one or more GPCRs and which exhibit desirable characteristics for the same.
WO2011047420A1 Cosmetic compositions A topical antimicrobial composition including (i) a polymer of 2-propenal, and (ii) a C3-10 alkanediol.
US20110110890 Novel Inhibitors of Hepatitis C Virus Replication The embodiments provide compounds of the general Formula I and compound 105S, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
WO2013061205A8 (4-phenylimidazol-2-yl) ethylamine derivatives useful as sodium channel modulators The invention relates to imidazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new imidazole Nav1.8 modulators of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. Nav1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.
US20080226616 Mixture comprising polyacrylic acid salts, acrylate/C10-30 alkyl acrylate crosspolymer and carrageenan for use as agent which reduces cellulite and skin irregularities The present invention relates to a cosmetic preparation containing an emulsifier combination of polyacrylic acid salts, acrylate/C10-30 alkyl acrylate crosspolymer and carrageenan and the use of the cosmetic preparation.
CN102875518A Genipin methyl ether, preparation method and medicine application thereof The invention relates to genipin derivatives, preparation methods and medicine applications thereof, and particularly relates to genipin methyl ether, preparation methods and medicine applications thereof; the genipin methyl ether comprises R-type genipin methyl ether, S-type genipin methyl ether, and a mixture of genipin methyl ether with the two configurations and with various proportions; the invention also discloses a preparation method of the R-type genipin methyl ether, the S-type genipin methyl ether, and the mixture of genipin methyl ether with the two configurations and with various proportions.
WO2007074871A1 Novel cxcr4 antagonist and use thereof Disclosed is a novel low molecular weight, non-peptidic CXCR4 antagonist prepared using various aromatic compounds each having a dipicolylamine-zinc complex. Also disclosed is use of the CXCR4 antagonist as an anti-HIV agent, a metastasis inhibitor for a malignant tumor or a therapeutic and/or prophylactic agent for rheumatoid arthritis.
WO2013018675A1 N-hetero-ring-substituted amide derivative The purpose of the present invention is to provide: a compound having an excellent hypoglycemic activity and an excellent activity of protecting β cells or the pancreas, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition having an excellent therapeutic and/or prophylactic effect on type-1 diabetes, type-2 diabetes and the like in which glucose metabolism disorders occur to induce the increase in blood glucose levels. A compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
US20050159333 Carbachol, neurokinin A, P2X receptor antagonist, electrical stimulus, to inhibit polypeptide in Rho associated kinase pathway; lower urinary tract disorders, overactive bladder Method for modulating bladder smooth muscle contractility comprising the step of contacting a polypeptide in a ROCK pathway with a compound that modulates an activity of said polypeptide.
WO2005013984A1 Selective serotonin reuptake inhibitors for the treatment of premature female orgasm The present invention provides the use of selective serotonin reuptake inhibitors (SSRIs) to treat premature female orgasm.
CN103127162A Application of scallop glycosaminoglycan in preparing dementia resistant medicine The invention relates to the field of medical technology, in particular to new application of scallop glycosaminoglycan in preparing a dementia resistant medicine. 5 to 100k of the scallop glycosaminoglycan is extracted and purified from skits of scallops which are marine organism. Experiments show that the scallop glycosaminoglycan can shorten an incubation period of a small rat with adementia caused by scopolamine before the rat steps on a platform, the number of platform penetration is increased, quadrant swimming time where the platform located is prolonged and study and memory capacity of small rat with the adementia caused by the scopolamine is improved. The scallop glycosaminoglycan has dementia resistant activity and can be used in preparing the dementia resistant medicine.
US20060211755 3-oxo-1, 3-dihydro-indazole-2-carboxylic acid amide derivatives as phospholipase inhibitors The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C5-C13alkyl; C,—C,2haloalkyl, C4C,2alkenyl, C4-C12alkynyl, or C,—C5alkylcycloalkyl, C3-C8cycloalkyl, C, C5alkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with one to three substituents independently selected from C,—C8a)kyl, C,—C8haloalkyl, ′C2-CBalkenyl, C2-C8a)kynyl, phenyl, benzyl, hydroxy, C,—C5 alkoxy, (C}12)m000C,—Csalkyl, (CH2)mNRaRb, and C,C4alkylcycloalkyl; wherein W and Rb are independently selected from hydrogen, C,CBalkyl, C2-CBalkenyl, C2-CBalkynyl, and C,—C5alkylcycloalkyl; R2 is hydrogen; R3, R4, R5, and R6, are independently selected from hydrogen, C,—C12alkyl, C2C,2haloalkyl, C2-C,2 alkenyl, C2-C12alkynyl, C,—C12alkylaryl, C,—C12alkylcyclohexyl, C, C12alkylcyclopentyl, C,—C12alkylheterocyclic, (CH2)m000H, (CH2)mC0(C,—C,o)alkyl, (CH2)m COO(C,—C,o)alkyl, (CH2)mCOO(C1-C,o)alkylaryl, C,—C,oalkylamino, halo, (CH2)mCONH2, (CH2)rCONRaRb, phenyl, or aryl wherein each of the phenyl or aryl groups is optionally substituted with one to three groups independently selected from CBalkyl, C,—CBhaloalkyl, C2-CBalkenyl, CZCBalkynyl, phenyl, benzyl, hydroxy, C,—C5 alkoxy, (CH2)m000C,—Csalkyl, and C,—C4alkylcycloalkyl; and wherein m is 0, 1, 2, or 3; R7 is selected from the group consisting of hydrogen, C,—Cloalkyl, C,C,ohaloalkyl, C2-C,oalkenyl, C2-C,oalkynyl, C,—C6alkylaryl, C,—C6alkylcyclohexyl, C—C6aikylcyclopentyl, C,—C6alkylheterocyclic, or aryl; or a pharmaceutically acceptable sallvate thereofi together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase-mediated diseases.
US20050171338 Mammalian tribbles signaling pathways and methods and reagents related thereto The invention provides methods and reagents for modulating mitogen activated protein kinase pathways using mammalian tribbles homologs (htrb).
WO2014093189A1 Methods of treating diabetes by administering a glucagon receptor antagonist in combination with a cholesterol absorption inhibitor Use of a glucagon receptor antagonist in combination with a cholesterol absorption inhibitor for the treatment of diabetes and related conditions is disclosed.
EP2223914A1 Tricyclic condensed pyrazole derivatives as CB1 inhibitors Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring rcomprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I) : wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.
CN1810236A Liposome preparation of garlicin One new kind of medicine preparation is formed through loading chemically synthesized garlicin onto liposome as new medicine carrier by means of reverse evaporation or film dispersing process. The medicine preparation is classified into long circulating liposome preparation of garlicin and common liposome preparation of garlicin according to whether the phosphatide molecule on the surface of the liposome is modified with polyglycol-distearoyl diphosphatidyl ethanolamine or not.
WO2009015812A3 Prodrugs of 2-amino-6- ( { [2- (4-chlorphenyl) -1, 3-thiaz0l-4-yl] methyl}thio) -4- [4- ( 2 -hydroxyethoxy) phenyl] pyridin-3, 5-dicarbonitrile The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridin-3,5-dicarbonitrile, process for the preparation thereof, the use thereof for the treatment and/or prophylaxis of diseases, and the use thereof for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders.
US20100015174 Method to control dengue viruses in humans by picolinic acid and derivatives thereof A method treats and then prevents a virus for afflicting an animal or a human as a metalloprotein mediates the virus. The method administers systemically a therapeutic pharmacological agent of picolinic acid either singly or with interferons, chemokines or cytokines to fight dengue fever virus. The picolinic acid inactivates the metalloprotein that allows replication of the virus. The picolinic acid has the structure of: where R1, R2, R3, and R4 are mutually exclusive. The viral proteins disintegrate by macrophage proteolytic enzymes stimulated by the picolinic acid.
CN101385701A Anticancer composition loaded with norcantharidin and galamustine An anticancer composite carrying norcantharidin and galamustine is a sustained release injection which consists of sustained release microspheres and a dissolvent, wherein, the sustained release microspheres comprise an anticancer active component and a sustained release adjuvant, and the dissolvent is a common dissolvent or a special dissolvent containing a suspending agent. The suspending agent has the viscosity of 100cp-3000cp (at the temperature of 20-30 DEG C), and is selected from sodium carboxymethyl cellulose and the like; the anticancer active component is a combination of a nitrosourea drug and an alkylating agent selected from melphalan, iphosphamide, 4H-peroxy-cyclophosphamide or norcantharidin; the sustained release adjuvant is selected from copolymer of polyphosphate esters p(LAEG-EOP), p(DAPG-EOP) and the like, or copolymer of the polyphosphate esters and polylactic acid, polifeprosan, dienoic fatty acid and sebacic acid, copolymer or polyblend of poly(erucic acid dimer-sebacic acid) or poly(fumaric acid-sebacic acid); the anticancer composite is also made into a sustained release implant, and injected into or placed inside or at the periphery of tumor to keep the effective drug concentration more than 60 days. The anticancer composite can also obviously reduce the general reaction of the drug, and selectively enhance the curative effects of non-operative therapies such as radiotherapy, chemotherapy and the like.
US20080194691 Apoptosis Promoters Compounds of formula (I), in which B1 and X1 are together alkylene which is unsubstituted or substituted with ═O and having one CH2 moiety unreplaced or replaced with CH═CH, O, NH or N(alkyl), which inhibit the activity of antiapoptotic Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases during which are expressed one or more than one of an anti-apoptotic family protein member are disclosed.
EP1241254B1 Apoptosis inhibitory polypeptide, gene and polynucleotide encoding it and compositions containing the same At least one serine residue in the amino acid sequence of wild type Bc1-2 protein is substituted by alanine or aspartic acid to give a polypeptide having a potentiated apoptosis inhibitory activity compared with the wild type Bc1-2 protein.
CN103520087A Policresulen expandable vaginal suppository, and preparation method and detection method thereof The invention relates to a policresulen expandable vaginal suppository, and a preparation method and a detection method thereof. The expandable vaginal suppository comprises a drug-containing matrix formed by policresulen and a matrix, and an expansion carrier. A diluent in the drug-containing matrix is in favor of dispersion of policresulen in the suppository and increase content uniformity of the suppository; the osmotic pump expandable vaginal suppository can realize the zero-level stable release of the policresulen, uniform and smooth performance of the drug effect of the suppository and prolong the action time of policresulen on the vagina; and the diluent can also promote the permeability of the policresulen. The policresulen expandable vaginal suppository provided by the invention employs seven originally created leading technologies and has beneficial effects of prevention of outflow liquid, high stability, lasting curative effect and prevention of secondary infection.
CN103463101A Application of Kadcoccitones A in preparing monoamine oxidase (MAO) inhibitor The invention provides application of Kadcoccitones A in preparing a monoamine oxidase (MAO) inhibitor. Compared with the existing MAO inhibitor, the Kadcoccitones A has greatly higher activity and selectivity for MAO-A and MAO-B. The application of the Kadcoccitones A in preparing the MAO inhibitor is disclosed for the first time; and the Kadcoccitones A has high activity for inhibiting MAO, has the characteristic of outstanding materiality, and apparently has marked progresses when being used for treating MAO maladjustment related diseases.
CN103159758A (1S,3S)-1-p-nitrophenyl-1,2,3,4-tetrahydro-beta-carboline acyl amino acid, and synthesis, antithrombotic activity and application as antithrombotic agent thereof The present invention discloses (1S,3S)-1-p-nitrophenyl-1,2,3,4-tetrahydro-beta-carboline acyl amino acid of a general formula, discloses synthesis thereof, in vitro anti-platelet aggregation activity thereof, and further discloses in vivo anti-thrombotic activity thereof in a rat thrombosis model. The present invention thus discloses the clinical application prospect of (1S,3S)-1-p-nitrophenyl-1,2,3,4-tetrahydro-beta-carboline acyl amino acid as an antithrombotic agent.
CN101780074B Anti-lung cancer pharmaceutical composition The invention discloses an anti-lung cancer pharmaceutical composition which is prepared by mixing four thiazolidone compounds, wherein the thiazolidone compounds are respectively 5-(4-dimethylamino benzylidene)-2-(o-methylphenyl-imido)-1,3-thiazole-4-ketone, 2-(2-methoxyphenyl-imido)-5-(4-dimethylamino benzylidene)-1,3-thiazole-4-ketone, 2-(3-trifluoromethyphenyl-imido)-5-(4-dimethylamino benzylidene)-1,3-thiazole-4-ketone, and 2-(3-fluorophenyl-imido)-5-(4-dimethylamino benzylidene)-1,3-thiazole-4-ketone, and the mixing ratio (mol ratio) of the four thiazolidone compounds is 1:1:1:1. The anti-lung cancer pharmaceutical composition of the invention can selectively kill human lung cancer cells H460 and H460/RT in vitro, has no obvious toxicity on normal fibroblast, has stronger drug effect in a drug resistant lung cancer cell line than that of a single thiazolidone compound, presents good synergic anti-cancer activity, and has better clinical application prospect.
US20080057113 virion vaccine anti-herpes simplex viruses containing hi-tech immunomodulator Polyoxidonium ( copolymer of 1,4-ethylene-piperazine N-oxide and (N-carboxyethyl)-1,4-ethylene-piperasinium bromide), valine, lysine together with metabolic amino acids; immunocompetent A new anti-herpetic composition is proposed which comprises a virion preparation containing herpes simplex viruses of serotypes 1 and 2 inactivated by formalin or γ-irradiation; the composition further comprises a hi-tech immunomodulator Polyoxidonium, and also amino acids valine and lysine, as well as a combination consisting of at least two amino acids selected from the group: phenylalanine, leucine, alanine, threonine, histidine, arginine, methionine, and can also comprise isoleucine, which is able to stimulate the formation of anti-herpetic peptides at the cell level. The composition can be formulated into various pharmaceutical forms, and owing to its properties it can be used not only in the case of acute, but also in the case of chronic herpetic pathology.
CN101612220B External-application cream for treating osteoarthritis and preparation method thereof The invention relates to and discloses a medicament for treating osteoarthritis and a preparation method thereof. Each 1000 grams of the external-application cream mainly comprises raw materials with the following components according to parts by weight: 20g to 30g of safflower, 45g to 55g of angelica, 45g to 55g of peach kernel, 45g to 55g of radix aconiti lateralis preparata, 45g to 55g of rhizoma ligustici wallichii, 18g to 22g of crude radix aconiti, 4g to 6g of prepared mastic, 4g to 6g of prepared myrrh, 8g to 12g of borneol and 4g to 6g of menthol. The external-application cream prepared by the invention can effectively improve the inflammation of the bone joints and peripheral synovial membranes, quickens the blood circulation, eliminates symptoms, such as gall, activity obstacle and the like, of the joint, relieves the state of an illness, has extremely few adverse reactions and is convenient for a patient to use and carry.
CN103505431A Repaglinide tablets The invention relates to repaglinide tablets and a preparation method thereof, belonging to the field of medicine technology. The repaglinide tablets are characterized by consisting of repaglinide, methyl cellulose, dicalcium phosphate anhydrous, microcrystalline cellulose, crosslinked sodium carboxymethylcellulose, magnesium stearate, meglumine and poloxamer.
US20120207766 Intracellular toll-like receptors pathways and axonal degeneration The present invention is directed to the identification of novel mechanisms involved in the initiation and spreading of axonal degeneration. In particular, the instant invention relates to the identification of a relationship between Toll-Like Receptors (TLRs) and axonal degeneration and the use of TLR inhibitors as antagonists of axonal degeneration.
US20080138317 Monoglycerides; polyethers; antidiabetic agents; rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, asthma, acute respiratory distress syndrome, chronic obstructive pulmonary disease, and multiple sclerosis The present invention relates to the use of bioabsorbable and biocompatible amphiphilic polymers as an anti-inflammatory agent. In particular, the present invention provides methods of treating inflammatory diseases or conditions by employing an amphiphilic polymer made of a polybasic acid or a derivative thereof, a monoglyceride and a polyether.
US20120276204 Bone Growth Compositions and Methods The present invention provides an improved technique for spinal fusion involving the administration of an HMG-CoA reductase inhibitor to a fusion. The HMG-CoA reductase inhibitor is preferably delivered to the site by a carrier. More preferably, the HMG-CoA reductase inhibitor is delivered to the site by a non-compressible delivery vehicle. The invention is suitable for promoting non-anatomic or heterotopic bone growth between any bony surfaces where bone growth is desired but does not naturally occur.
US7199136 Antiinflammatory agents, neutrophil elastase inhibitors; chronic obstructive pulmonary diseases The invention relates to novel 1,4-dihydro-1,4-diphenylpyridine derivatives of formula (I) wherein the variable groups are as defined in the text and claims. Processes for their preparation, pharmaceutical compositions containing them, and methods of treatment of inflammatory processes, expecially chronic obstructive pulmonary diseases, using them are also disclosed and claimed.
US20110038832 Method for treatment of macular degeneration using (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione Provided herein are methods of treating macular degeneration, which comprises administering to a patient in need thereof a therapeutically effective amount of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, or a pharmaceutically acceptable salt or solvate thereof.
CN101554415A Anti-acne toner and preparation method thereof The invention relates to an anti-acne toner and a preparation method thereof. The anti-acne toner is prepared by the following ingredients: sulfur, angelica dahurica, snakegourd fruit root, scorpion, raw rhubarb, radix scutellariae, rhizoma coptidis, orostachys fimbriatus and fructus gleditsiae. The anti-acne toner has simple formulation and low cost, and can effectively treat acne, without side effects.
US20120225933 Regulated expression systems The application relates to gene constructs for inducible hepato-specific expression of polynucleotides of interest in response to an inducer agent, said constructs comprising (i) an inducible bi-directional operator-promoter with at least one responsive element to said inducer agent flanked by two hepato-specific promoters acting in divergent manner, (ii) a first nucleotide sequence encoding a transactivator which may be activated by said inducer agent operatively coupled to the first hepato-specific promoter and (iii) a second nucleotide sequence operatively coupled to the second hepato-specific promoter, wherein the promoters are induced as a consequence of the binding of the transactivator to the operator region of the operator-promoter in the presence of the inducer agent.
US20110086812 Transition state sturcture of 5'-methylthioadenosine/s-adenosylhomocysteine nucleosidases Provided are methods of designing a putative inhibitor of a 5′-methylthioadenosine/S-adenosylhomocysteine nucleosidase. The methods comprise designing a chemically stable compound that resembles the charge and geometry of the 5′-methylthioadenosine/S-adenosylhomocysteine nucleosidase transition state. Also provided are methods of inhibiting 5′-methylthioadenosine/S-adenosylhomocysteine nucleosidases using the inhibitors found by the above methods.
US20100093654 Tetrasubstituted clucopyranosylated benzene derivatives, medicaments containing such compounds, their use and process for their manufacture Tetrasubstituted glucopyranosylated benzene derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
CN103585161A Medicinal composition, and its application in preparation of medicines for treating obesity, insulin resistance and diabetes The invention discloses a medicinal composition and its application in the preparation of medicines for treating obesity, insulin resistance and diabetes. The medicinal composition containing sodium salicylate and oleanolic acid is injected to the abdominal cavity of a diabetic animal to substantially reduce the blood sugar level, and the composition containing sodium salicylate and oleanolic acid is added to a culture solution of differentiated 3T3-L1 adipocytes to substantially inhibit the tumor necrosis factor induced insulin signal disorder, so the composition containing sodium salicylate and oleanolic acid can be used in medicines for treating the obesity, the diabetes, the insulin resistance, and insulin resistance closely related metabolic syndromes.
CN101209109B Composition with muscle-increasing function and beverage prepared thereby The invention provides a composition with the muscle strengthening function, which takes whey protein and carbohydrate to compose the main ingredients according to the scientific proportion, the invention can also be supplemented with creatine, various amino acids, chromium and a small amount of fat, and can further be added with vitamin B6 and dietary fiber. The administration of the muscle strengthening composition can significantly increase the lean body weight, does not increase or less increases the body fat and improves the maximum strength of the muscle, wherein, the maximum strength is the maximum value of the muscle which is represented by the maximal voluntary contraction overcoming resistance.
CN101991554B Bergenin osmotic pump tablet and preparation method thereof The invention provides a bergenin osmotic pump tablet. The bergenin osmotic pump tablet is prepared by coating bergenin, a penetration enhancer and an auxiliary material suppressant tablet core with a controlled release film and punching, wherein the penetration enhancer is polyethylene oxide PEO and mannitol, the tablet core contains 8.3-37.5wt% of bergenin, 3.5-45wt% of polyethylene oxide PEO and 20-45wt% of mannitol. The invention also provides a preparation method of the bergenin osmotic pump tablet. The invention improves the solubility of a slightly soluble drug of the bergenin by utilizing a Beta-cyclodextrin inclusion technology, and further the bergenin is prepared into a single layer osmotic pump type controlled release tablet so as to decrease the drug release speed, reduce thedosage frequency, improve the bioavailability and greatly simplify the process; compared with the common bergenin tablet, the solubility of the prepared bergenin solid dispersoid osmotic pump tablet is obviously enhanced, and the drug is released according to a zero order release speed, and the blood drug level is more moderate and stable, thereby improving the bioavailability, enhancing the clinic curative effects, reducing the dosage frequency and increasing medicine-taking compliance of a patient so that the bergenin is applied more widely in medicine.
CN101394868B Strong immune induction by using combination of adenovirus type-5/type-35 vector and vaccinia virus mva vector Disclosed is an effective and inexpensive anti-HIV agent. The anti-HIV agent comprises a combination of a recombinant viral vector having the structural gene of HIV inserted into a chimeric virus and a recombinant viral vector having the structural gene of HIV inserted into a modified vaccinia virus Ankara, wherein the chimeric virus is prepared by substituting a fiber in an adenovirus type-5 by a fiber derived from an adenovirus type-35.
CN100584335C Composition and uses for treatment of reactive arthritis or bursitis A pharmaceutical formulation for treating conditions in human beings associated with either or both reactive arthritis or bursitis comprising a combination of acyclovir, minocycline, hydrochloride, and metronidazole. An alternate treatment comprises the combination of valacyclovir hydrochloride , minocycline hydrochloride, and metronidazole.
CN101810679A Polyunsaturated fatty acid soft capsule and preparation method thereof The invention relates to a polyunsaturated fatty acid soft capsule which comprises a soft capsule shell and content. The content comprises the following effective ingredients in percentage by weight: 7.6-8.8 percent of linolenic acid, 49.0-60.0 percent of linoleic acid, 7.0-12.9 percent of oleic acid, 0.25-0.5 percent of ganoderma triterpene and 1.6-3.0 percent of vitamin E and the balance of reagent capable of being accepted by the human body. Proved by animal functions and human body test eating experiments, the polyunsaturated fatty acid soft capsule has a health care function for improving the sleep quality, and also has a health care function of oxidation resistance.
CN102018668A Preparation method of aceglutamide The invention provides a preparation method of aceglutamide. By utilizing the new method provided by the invention, the defect of the relevant substances of the aceglutamide due to the existing method can be overcome. In the method, the temperature of 70-80 DEG C of the prepared water for injection is improved into the water temperature of 35-42 DEG C; and after the product is subjected to detection, an accelerated test, a long term stability test and the like, a data result shows that all indexes of the relevant substance, content and the like of the aceglutamide can reach the standard of the China Pharmacopeia 2010 edition after the new method provided by the invention is adopted. The method provided by the invention is simple and practicable and is suitable for industrial production on a large scale.
CA2214531C Treatment of cytokine growth factor caused disorders In preferred embodiments, a method of prevention and treatment of disorders caused by enhanced proliferation and enhanced biosynthesis caused by cytokine growth factors in humans and other animals, the method including: administering to a human or other animal an effective dose of a pharmaceutical substance including an N-substituted 2(1H) pyridone and/or an N-substituted 3(1H) pyridone;and a composition for prevention and treatment of disorders caused by enhanced proliferation and enhanced biosynthesis caused by cytokine growth factors in humans and other animals, the composition including: a pharmaceutical preparation including an effective dose of an N-substituted 2(1H) pyridone and/or an N-substituted 3(1H) pyridone.
CN102342911A Ganciclovir eye drops and preparation method thereof The invention aims at providing a ganciclovir antiviral new medicament for eye with high efficiency, low toxicity, strong selectivity and good stability, and a preparation method thereof. The medicament provided by the invention comprises 0.1wt% of ganciclovir used as a main medicament, and a cosolvent, an iso-osmotic regulator, a pH regulator, a preservative and water for injection used as auxiliary agents. Compared with the prior art, the medicament has the following advantages that: a boric acid buffer, namely a mixed solution of boric acid and borax is adopted, and the buffer has strong buffering capability and is highly soluble in water; and poloxamer is selected as the cosolvent, and multiple data show that the poloxamer improves the inherent quality of the medicament, increases the preparation stability, reduces the irrigation of anti-inflammation analgesic to eyes, has no hemolysis action as compared with tween-80, has no interference to the bacteriostatic action of the preservative, and has very significant effect on reducing the irritation of medicament to eyes.
CN1823770A Compound Dextromethorphan oral cavity disintegration tablet A compound oral disintegrating tablet of dextromethorphan for treating the cough of baby is prepared from loratadine, dextromethorphan or its hydrobromate, and the pharmacologically acceptable additives including filler, disintegrant, adhesive or wetting agent, lubricant, flavouring and coloring agent.
EP1830850B1 Quinoline derivatives for the treatment of latent tuberculosis Use of a compound of formula (Ia) or (Ib) for the manufacture of a medicament for the 5 treatment of latent tuberculosis, wherein the compound of formula (Ia) or (Ib) is a pharmaceutically acceptable salt, a quaternary amine, a N-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula (II); R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is zero, 1, 2, 3 or 4; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl ; or two vicinal R6 radicals may be taken together to form a bivalent radical -CH=CH-CH=CH-; r is 1, 2, 3, 4 or 5 ; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 together form the radical =N-CH=CH-.
EP1682565A1 Iap nucleobase oligomers and oligomeric complexes and uses thereof The present invention provides nucleobase oligomers and oligomer complexes that inhibit expression of an IAP polypeptide, and methods for using them to induce apoptosis in a cell. The nucleobase oligomers and oligomer complexes of the present invention may also be used to form pharmaceutical compositions. The invention also features methods for enhancing apoptosis in a cell by administering a nucleobase oligomer or oligomer complex of the invention in combination with a chemotherapeutic or chemosensitizing agent.
EP1392256B1 Improved transdermal therapeutic system for the treatment of parkinson's disease This invention provides the use of a silicone-based transdermal therapeutic system having an area of 10 to 40 cm<2> and containing 0.1 to 3.15 mg / cm<2> of Rotigotine as active ingredient, for the preparation of an anti-Parkinson medicament which effects an improvement, compared to a placebo treatment, of the condition of human Parkinson patients, measured according to the Unified Parkinson's Disease Rating Scale (UPDRS) parts II and III, of 2 units or more following administration for a time period of at least 7 weeks.
WO2008024980A3 Pyrrole, thiophene, furan, imidazole, oxazole, and thiazole derivatives Disclosed are compounds and pharmaceutically acceptable salts of Formula (I) wherein RQ, R7, n, Q2, Q3, Y, and X1-X3 are as defined herein. Compounds of Formula (I) are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
US6887871 Use of phenylheteroakylamine derivatives There is disclosed the use of a compound of formula (I) wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy. The compounds of formulae (I) and (Ia) are inhibitors of the enzyme nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease.
US20080027109 CETP Activity Inhibitors The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof. The compounds represented by the formula (I) can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity and, therefore, is expected to be useful as a new type of a preventive or therapeutic agent for atherosclerosis or hyperlipidemia.
WO2009142569A1 Phenyl or pyridinyl substituted indazoles derivatives A compound of formula Ia: Formula (la) The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments.
EP2634173A1 Polymorph of n-(6-(4-chlorophenoxy)hexyl)-n'-cyano-n''-(4-pyridyl)guanidine, and preparation therefor and use thereof Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N'-cyano-N"-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
US20120232135 (-)-Epigallocatechin Gallate Derivatives for Inhibiting Proteasome A method of reducing tumor cell growth, the method including administering an effective amount of a compound having the formula:
EP2150551A1 2-oxo-3-benzyl-benzoxazol-2-one derivatives and related compounds as met kinase inhibitors for the treatment of tumors The invention relates to compounds of formula (I), wherein R1, R2, R3, R3', R4, R4', E1 E', E', and E'' have the meaning stated in claim (1) that are inhibitors of tyrosine kinases, particularly of Met kinase, and can be utilized, among other things, for the treatment of tumors.
WO2005009471A1 Composition for lowering blood-sugar level The present invention provides compositions, which have an action to lower blood sugar levels in subjects in a hyperglycemic state based on a mechanism that is different from conventional drugs to treat diabetes, and which are used for lowering the blood sugar levels of the subjects. The present invention also provides compositions to prevent or treat diseases caused by hyperglycemia, specifically, diabetes and the complications of diabetes, based on the action above. The invention further provides a method to lower blood sugar levels of subjects in a hyperglycemic state, and a method to prevent or threat diseases caused by hyperglycemia, using a hypoglycemic action based on the novel mechanism of action of the composition. The present invention also provides a method to screen the active ingredient of the above compositions. The present invention provides novel imidazole compounds represented by formula (1), which has an action of lowering the blood sugar level of a subject in a hyperglycemic state, and is useful as an active ingredient of a hypoglycemic composition, or an active ingredient of a composition that can be used for preventing or treating disorders caused by hyperglycemia, specifically diabetes and complications of diabetes.
EP2621493A1 N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A 2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
CN102675107A Glyceride compounds with anti-inflammatory activity, and preparation method and application thereof The invention relates to glyceride compounds with anti-inflammatory activity, and a preparation method and application thereof. The preparation method comprises the following steps: acquiring an extractive from propolis, conventionally carrying out silica gel reduced pressure column chromatography, carrying out gradient elution with a petroleum ether (60-90 DEG C)-acetone system, merging the eluates according to the analytic result of thin-layer chromatography, and separating to obtain the glyceride compounds. The in-vitro anti-inflammatory activity test proves that the glyceride compounds can obviously inhibit the expression levels of IL-1beta, IL-6 and COX-2mRNA in the mouse macrophage RAW 264.7 caused by lipopolysaccharide (LPS), and have a dosage dependency relationship, which indicates that the glyceride compounds have obvious anti-inflammatory activity. The invention can be used for preparing new anti-inflammatory activity medicines.
CN101406449A Compound dichlofluanid injection and technique for preparing the same The invention discloses compound recipe fluorobenzene sulfanilamide injection and a preparation process thereof. The injection comprises the following components: florfenicol, PVP polyvinylpyrrolidone k30, sulfanilamide-5-oxymethylpyrimidine sodium or sulfanilamide-6- oxymethylpyrimidine sodium, TMP, N,N-dimethylformamide, propylene glycol, sodium sulfite, EDTA, and 95 percent ethanol. The preparation process comprises the following steps: (1) dissolving the florfenicol in the N,N-dimethylformamide; (2) taking the propylene glycol, adding the TMP into the propylene glycol and stirring the mixture till the TMP is completely dissolved, and adding the ethanol into the mixture; and (3) taking water for injection, adding sulfonamide into the water and stirring the water till sulfonamide is dissolved, and adding 1N NaOH fluid, the PVP k30, and the like into the mixture. The compound recipe fluorobenzene sulfanilamide injection has the advantages that the compound recipe fluorobenzene sulfanilamide injection is a compound recipe preparation, containing the florfenicol and doxycycline, can widen the application range, and reduce the dosage of the florfenicol and the production and application cost.
EP2077849A1 Use of compounds of the avermectin family for the treatment of dermatological disorders in human beings The present invention relates to the use of compounds of the avermictin family or derivatives thereof for producing a pharmaceutical composition for the treatment of dermatological affections in human beings, in particular rosacea.
US20080269231 Phenazine Compounds and Use Thereof in Autoimmune and Inflammatory Disease The invention discloses compounds, compositions and methods useful for preventing and/or treating autoimmune diseases and inflammatory diseases. The methods and compositions utilize water-soluble phenazine compounds, or salts, or solvates thereof. These molecules can be delivered alone or in combination with agents which treat or prevent autoimmune diseases and inflammatory diseases such as those caused by arthritis and rheumatoid arthritis.
US20110008447 Carrier comprising nanodiamond The present invention provides a carrier including a nanodiamond (ND) particle and a linker covalently bound to the ND particle, in which the linker is presented by the formula: —R1—O(R2)m-Q-. In addition, the present invention further provides a carrier having an active unit covalently bound to the linker, in which the active unit is a drug, a vitamin or a biological molecule.
US7045525 Use of (R)-peniciclovir triphosphate for the manufacture of a medicament for the treatment of viral diseases A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.
CN101953821A Medicinal composition taking levalbuterol and ambroxol as main active ingredients The invention discloses a medicinal composition taking levalbuterol and ambroxol as main active ingredients and relates to the medicinal composition taking the levalbuterol and the ambroxol as active ingredients. Compared with salbutamol, the levalbuterol has better curative effect and smaller side effect.
US20120196815 Withanolide Isolated from Physalis longifolia and Analogs and Methods of Use Thereof The present invention features novel withanolides, as well as analogs and salts thereof, for use in the treatment of proliferative disease, cardiovascular disease, neurodegenerative disease and inflammatory disease.
WO2012130141A1 Method and composition for enhancing target cells uptake of therapeutic agents The present invention provides a method and composition for elevating the therapeutic efficacy of therapeutic agents by enhancing target cells uptake of the therapeutic agents, wherein the composition contains regulator having caveolae/lipid rafts dependent endocytic pathways, wherein the therapeutic agents are such as antitumor drugs. The invention also relates to a composition comprising regulator that have caveolae/lipid rafts dependent endocytic pathways and therapeutic agents. The invention further relates to a method for screening regulator having lipid rafts-caveolae dependent endocytic pathways which could enhance the therapeutic efficacy of antitumor drugs.
WO2012095433A1 Compositions comprising 2-chloro-n- (4 - chloro - pyridin- 2 - yl - phenyl) - 4 -methanesulfonyl - benzamide and 2, 2 -dimethyl -n- ( (s) - 6-0x0-6, 7 - dihydro - 5h - dibenzo [b, d] azepin-7 -yl) -n' - (2,2,3,3,3- pentafluoro - propyl) malonamide The present invention relates to a combination therapy of 2-Chloro-N-(4-chloro-pyridin-2-yl-phenyl)-4- methanesulfonyl- benzamide and 2,2-Dimethyl-N-((S)-6-oxo-6,7-dihydro-5H- dibenzo[b,d]azepin-7-yl)-N'-(2,2,3,3,3-pentafluoro-propyl)-malonamide for treating a patient suffering from a proliferative disorder.
WO2007128761A3 Uses of dpp-iv inhibitors Disclosed is the use of selected DPP-IV inhibitors for treating physiological functional disorders and reducing the risk of at-risk patient groups developing such functional disorders. Also disclosed is the use of said DPP-IV inhibitors in combination with other agents such that improved treatment results can be obtained. Said uses can be employed for producing corresponding medicaments.
USRE40882 High concentration of alpha, beta or gamma interferon in buffered solution with polyvinylpyrrolidone and/or polyethylene oxide, and antioxidant, Trilon B (disodium salt of ethylenediaminetetraacetic acid); bioavailability; topical administration to mucous membrane with prolonged contact; bioavailability The present invention can be used in pharmacology specifically in the preparation of interferon-containing compositions, which are capable of conserving their biological activity and can be administered intranasally, e.g. in the preparation of nasal drops. This invention essentially refers to an antiviral agent in the form of nasal drops that contains a genetically engineered alpha, beta or gamma interferon with a viscosity of (1.1−30.0)* 10 10−3 Pascal .second, a biocompatible polymer and a buffer mixture. The agent may further include an antioxidant, and the ingredients are contained in the following amounts per ml buffer mixture: 1,000 to 5,000 500,000 IU of genetically engineered interferon; 0.005 to 0.714 g of biocompatible polymer; and 0.0001 to 0.0008 g of an antioxidant. TRILON B® (disodium salt of EDTA) is used as the antioxidant, whereas polyvinylpyrrolidone and/or polyethylene oxide is (are) used as the biocompatible polymer(s) at polyvinylpyrrolidone/polyethylene oxide ratio of 1:1-50.
CN1935153A Lyophilized powder injection containing three B-vitamins and its preparing method The present invention belongs to the field of medicine technology, in the concrete, it relates to a freeze-dried powder injection preparation containing three vitamins of B group and its preparation method. It is characterized by that in the freeze-dried powder injection preparation a proper quantity of supporting agent (excipient) is added, the resolubility of said freeze-dried powder injection preparation can be effectively improved, and the chemical stability of vitamin B6 and vitamin B12 can be obviously raised. Said product can be used for preventing and curing several diseases of nerve injury, polyneuritis, prosopalgia, sciatica and others.
WO2005023234A1 Molecules exhibiting anti-adipogenic activity on adipocyte human cells The invention relates to the use of a nordihydroguaiaretic acid (C18H22O4) or the derivative thereof as an active principle for a cosmetic or food composition in the form of a human adipocytes formation inhibitor or as an active principle for a derma-pharmaceutical or pharmaceutical composition for preparing a drug used for treating or preventing pathologies which provoke the adipocytic differentiation dysfunction of a human being.
CA2633243C Azepinoindole derivatives as pharmaceutical agents The present invention relates to compounds of formula I, which exhibit affinity for the farnesoid X receptor.
US7846435 Humanized antibodies that recognize Verotoxin II and cell line producing same The invention provides humanized antibodies that specifically bind to, and preferably, neutralize, verotoxin II (VT2). The antibodies are useful for treating patients suffering from, or at risk of suffering, toxic effects of verotoxin.
US20080260871 Method and composition for infusing herbal extracts and pharmaceuticals through the skin A topical mixture, that when massaged onto the skin, enables infusion of drugs or herbal compounds into deeper tissues, and a method of enhancing the penetration and concentration of drugs and herbs into tissues, especially as relates to treatment of pain.
EP1928840B1 1H-Pyrazole-4-carboxamides, their preparation and their use as 11-beta-hydroxysteroid dehydrogenase inhibitors Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II dia- betes mellitus and metabolic syndrome.
US20110046148 Spirocyclic Heterocycles Medicaments Containing Said Compounds, Use Thereof And Method For Their Production The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.
US20110230547 Potential Prognostic Markers and Therapeutic Targets for Neurological Disorders We recently found that Satb1 is expressed highly by mature neurons in specific regions of the postnatal brain. Satb2, a homolog of Satb1, is expressed at low levels in the postnatal brain. Neurons respond to external stimuli and rapidly and dynamically change their expression. Satb1 has been found to directly regulate a set of genes in the postnatal brain, presumably playing a crucial role as a ‘genome organizer’ for brain function and behaviors. Satb2 may also have a similar function, even though it is expressed at low levels in the postnatal brain. The present invention describes compositions, reagents and tools using wild type and variant SATB1 and SATB2 genes and proteins for use in diagnosis, prognosis and therapeutics in neurological dysfunction and psychiatric disorders.
EP1200446B1 OXATHIEPINO 6,5- i b /i ]DIHYDROPYRIDINES, AND RELATED COMPOSITIONS AND METHODS This invention provides novel oxathiepino[6,5-b]dihydropyridines. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.
US8552040 Isoxazoline compounds having MIF antagonist activity Methods of use and pharmaceutical compositions for a genus of low molecular weight compounds comprising optionally substituted isoxazoline ring systems that act as inhibitors of MIF (macrophage migration inhibitory factor) are disclosed. Specifically, the compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases (including rheumatoid arthritis, insulin-dependent diabetes, multiple sclerosis, graft versus host disease, lupus syndromes), asthma, arthritis, ARDS, psoriasis, interleukin-2 toxicity, proliferative vascular disease, and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization (angiogenesis).
US7244717 Mutagenic nucleoside analogs for the treatment of viral disease The present invention relates to methods of treating viral disease using mutagenic nucleoside analogs. In particular, the invention provides 5-aldehydo-uracil nucleosides and derivatives thereof, and methods of administration thereof to increase the virus mutation rate in a virally infected cell.
WO2006073126A1 Preventive and remedy for dry eye associated with chronic graft versus host disease It is intended to provide a medicinal composition for preventing and treating dye eye associated with chronic graft versus host disease (cGVHD) following the transplantation of hematopoietic stem cells. Namely, a medicinal composition or the like for preventing and treating dye eye associated with GVHD occurring after the transplantation of hematopoietic stem cells such as peripheral blood stem cell transplantation, cord blood transplantation or bone marrow transplantation which contains as the active ingredient N-(3,4-dimethoxycinnamoyl)anthranilic acid (common name: tranilast) or a pharmacologically acceptable salt thereof.
WO2013157005A1 Methods and compositions for treating viral infections The present invention provides compositions and methods for treating, preventing, and inhibiting viral replication, viral infections and viral diseases and disorders, comprising the use of artemisinin derivatives having anti-viral activity.
CN103169695A Application of alpha-lipoic acid, acetyl-L-carnitine, coenzyme Q10 and hydroxytyrosol composition for preventing and treating amyotrophy The invention relates to an application of an alpha-lipoic acid, acetyl-L-carnitine, coenzyme Q10 and hydroxytyrosol composition for preventing and treating amyotrophy, wherein the alpha-lipoic acid, the acetyl-L-carnitine, the coenzyme Q10 and the hydroxytyrosol are composited in appropriate proportion, so that the generation of mitochondria in muscle can be promoted; the loss of the mitochondria can be inhibited; and the muscle function can be improved. Therefore, the atrophy of muscle fibers during the generation process of the amyotrophy is inhibited effectively; and the growth of the muscle fibers during the recuperation process of the amyotrophy is promoted. In addition, the motion function decline caused by the amyotrophy is lightened effectively; and the improvement in the motion function during the recuperation process of the amyotrophy is promoted.
WO2007071363A3 METHODS OF USING THE CALCINEURIN A VARIANT Cnaβ1 The present invention relates to an inhibitor or activator of the calcineurin subunit Aβ1 isoform (CnAβ1) and the production of a medicament for the treatment of skeletal muscle injury or degeneration or cancer in a subject. CnAβ1 is constitutively active, cyclosporin-insensitive, highly expressed in proliferating myoblasts and human tumors, where it inhibits FoxO transcription factors independently of its phosphatase activity. The CnAβ1 isoform is a candidate for interventional strategies in muscle wasting, and a target for cancer treatment.
WO2009044895A1 Composition inhibiting the expression of target gene To provide a composition or the like having an effect of inhibiting the expression of a target gene and containing a microRNA or its derivative. Namely, it is intended to provide a composition or the like containing a liposome having a microRNA, an artificial microRNA, etc. encapsulated therein, which comprises a complex particle comprising a lead particle and the microRNA, artificial microRNA, etc. as described above together with a bimolecular lipid membrane coating the complex particle, wherein the component constituting the bimolecular lipid membrane is soluble in a specific polar organic solvent and the component constituting the bimolecular lipid membrane and the complex particle are dispersible in a liquid containing the polar organic solvent at a definite concentration.
US6869942 Comprises formoterol and corticosteroid; for use in treatment of respiratory disorders such as asthma, rhinitis and chronic obstructive pulmonary disease Inhalable pharmaceutical compositions are provided, for use in the treatment of respiratory disorders such as asthma, rhinitis and chronic obstructive pulmonary disease (COPD). These compositions have high storage stability, and include formoterol and a corticosteroid.
WO2006040047A2 Diagnostics and therapeutics for diseases associated with rho/rac-interacting citron kinase (cit) The invention provides a human CIT which is associated with cardiovascular diseases, respiratory diseases, dermatological diseases, endocrinological diseases, metabolic diseases, inflammation, gastroenterological diseases, cancer, hematological diseases, muscle skeleton diseases, neurological diseases, urological diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular diseases, respiratory diseases, dermatological diseases, endocrinological diseases, metabolic diseases, inflammation, gastroenterological diseases, cancer, hematological diseases, muscle skeleton diseases, neurological diseases, urological diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of CIT as well as pharmaceutical compositions comprising such compounds.
WO2009043114A1 Arsenoxide compound and method of use The present invention relates to organic arsenoxide compounds, pharmaceutical compositions comprising these compounds, and to their use in therapy, in particular treatment of proliferative diseases.
CA2816321A1 Compositions and methods for inhibition of pcsk9 genes The invention relates to siRNAs targeting a PCSK9 gene, and methods of using siRNAs to inhibit expression of PCSK9 and to treat PCSK9 related disorders, e.g., hyperlipidemia.
WO2009100116A1 Oligodendrocyte precursor cell composition and methods of use The present invention provides a cell culture enriched for sphingolipid enhances neural stem cells (SENSe), particularly oligodendrocyte precursor cells (ODPCs), that do not form teratomas after transplated in vivo. Methods for producing and use of the invention ODPCs or the cell culture enriched with these ODPCs for stem cell therapy are also provided. The invention method comprises culturing a stem cell culture with a cell culture medium comprising a ceramide compound and a SlP receptor agonist in sequence, overlapping intervals or concurrent manners. The present invention further provides a therapy using a composition comprising a ceramide compound in conjunction with a SlP1 agonist to proliferate or differentiate endogenous neural stem cells to ODPCs and further to oligodendrocytes.
US20120107383 Osteoconductive matrices comprising calcium phosphate particles and statins and methods of using the same Osteoconductive matrices and methods are provided that have one or more statins disposed in calcium phosphate particles. The matrices may be injected into a fracture site. The osteoconductive matrices provided allow for sustained release of the statin and facilitate bone formation and repair of the fracture site.
WO2009044548A1 Antidiarrhetic composition, product containing the same and method of preventing diarrhea To provide an antidiarrhetic composition which is efficacious against diarrhea, in particular, the predominant secretory diarrhea; an antidiarrhetic medicinal composition containing the same; a food containing the antidiarrhetic composition; and a method of preventing diarrhea using the same. [MEANS FOR SOLVING PROBLEMS] A composition for relieving diarrhea which is a cool composition capable of acting on the digestive tract in the recipient's body and inhibiting the secretion of the intestinal Cl-. In other words, a composition containing one or more kinds of cool act compounds. It may be provided by adding to medicines, foods or drinks.
US20090208486 Pharmaceutical composition comprising cxcr3 inhibitor A pharmaceutical composition for the treatment of cancer of which survival and/or metastasis is under the influence of signal transduction mediated by a chemokine receptor CXCR3, which comprises an agent to inhibit CXCR3, and a method of treatment and diagnosis of such cancer.
EP1608361A2 Compositions of cyclooxygenase-2 selective inhibitors and 5-ht1b/1d agonists for the treatment and prevention of migraine The present invention provides compositions and methods for the treatment of migraine. More particularly, the invention provides a combination therapy for the treatment of migraine comprising the administration to a subject of a 5-HT1B/1D agonist in combination with a cyclooxygenase-2 selective inhibitor.
WO2013057741A3 Pharmaceutical compositions of ursodeoxycholic acid The present invention is directed to pharmaceutical compositions of Ursodeoxycholic acid, wherein the composition comprises micronized Ursodeoxycholic acid having a particle size of d90 less than 25 microns and one or more pharmaceutically acceptable excipients.
CN103705470A Methylprednisolone-loading nanoparticles as well as preparation method and application thereof The invention discloses methylprednisolone-loading nanoparticles which consist of methylprednisolone and a carrier at a weight ratio of 1:(2-20), wherein the carrier is ibuprofen-modified ibuprofen and the grain size of the methylprednisolone-loading nanoparticles is 70-400nm. The invention further discloses a preparation method and application of the nanoparticles. The methylprednisolone-loading nanoparticles disclosed by the invention can be used for effectively transferring methylprednisolone to the injured part in a targeting manner, and have a very strong methylprednisolone slow-release function, so that side effects caused by high dosage and toxicity of methylprednisolone are avoided.
US20060069092 Pharmaceutical compositions for the treatment of diseases related to neurotrophines The present invention refers to pharmaceutical preparations including as active compounds 3-aza-bicyclo[3.2.1]octane derivatives of general formula (I) and/or their dimers of general formula (II) and (III) acting as agonists of human neurotrophines. Therefore, such compounds of formula (I), (II) and (III) are useful for treatment of diseases in which the neurotrophine functions are involved in defect, particularly of Nerve Growth Factor (NGF), such as neurodegenerative diseases of central nervous system (CNS), acquired immunodeficiency due to a reduced NGF biodisponibility, or morbous conditions in which the stimulus of neoangiogenesis process is convenient.
WO2010018133A1 Purine derivatives for use in the treatment of allergic, inflammatory and infectious diseases Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
CN101402982A Mud snail glue polysaccharide, preparation method and application thereof The invention belongs to the field of deep processing of aquatic products, in particular relates to a mollusk mucus polysaccharide and a preparation method thereof, the polysaccharide powder is prepared by taking mucus of living yellow mud snails as raw material, the yield of the crude polysaccharide is 5 percent-9 percent, the yield of the polysaccharide after the purification is 1 percent-3 percent, and the weight of the yellow mud snail mucus polysaccharide which is measured by the phenol-sulfuric acid method is 82 percent-90 percent. The production process comprises extraction, concentration, sedimentation, purification, separation, drying and other steps. The mucus polysaccharide of the provided product has higher effect of inhibiting tumor cell proliferation and black pigment formation. The provided production process is simple and has universal adaptability for the mucus extraction of living mollusk; furthermore, the extraction rate of the polysaccharide is high and the purity is high.
WO2009008362A1 Method for producing composition containing sialic acid compound It is intended to provide a method for producing a composition containing a sialic acid compound with a significantly high content of a sialic acid compound efficiently and economically from milk, whey, a processed product thereof or the like, which is a natural raw material containing a sialic acid compound. The method for producing a composition containing a sialic acid compound comprising using a liquid raw material containing a sialic acid compound or a liquid obtained by dissolving or suspending a solid raw material containing a sialic acid compound in water as a raw material, culturing, in the raw material, a microorganism which does not have an ability to assimiate a sialic acid compound and has an ability to assimilate a carbohydrate other than a sialic acid compound contained in the raw material, and removing the microorganism after the carbohydrate other than the sialic acid compound contained in the raw material has been assimilated is provided.
WO2009008303A1 Process for production of optically active mirtazapine Disclosed is a process for producing optically active mirtazapine with a high degree of efficiency. Specifically disclosed is a process for producing optically active mirtazapine by optically resolving an R/S mixture of mirtazapine with optically active tartaric acid in the presence of a solvent. More specifically disclosed is a process for producing optically active mirtazapine, which is characterized by contacting an R/S mixture of mirtazapine with optically active tartaric acid in the presence of a solvent to thereby crystallize a salt of optically active mirtazapine preferentially. The solvent is preferably a mixed solvent of a water-soluble organic solvent and water, more preferably a mixed solvent of an alcohol solvent having 1 to 3 carbon atoms and water.
US20090062269 Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
CN102028852A New purpose for compound aloes and new purpose-based medicament The invention belongs to the field of pharmacy, and relates to a new purpose for compound aloes, a new purpose-based medicament, new use of the compound aloes in the preparation of medicaments for treating or preventing hyperlipidemia with cerebral infarction. The compound aloes can improve the hemorheological indexes of patients obviously, relieve the expression of the hyperlipidemia with cerebral infarction effectively, and improve the neural function, so the compound aloes are favorable for the recovery of the integral bodies of the patients from illness.
US7560458 Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors This invention concerns compounds of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof, their use, pharmaceutical compositions comprising them, and processes for their preparation.
CN102793781A Anti-depression medicinal composition The invention relates to an anti-depression composition which comprises a centella extract, a morida officinalis how polysaccharide extract, citalopram and/or escitalopram. The composition can be used for preparing various medicinal preparations, such as solid preparations and/or liquid preparations, wherein the solid preparations comprise tablets, granules, capsules, drop pills, soft capsules and the like; and the liquid preparation comprises an oral solution, an injection, injection powder and the like. The medicinal composition which is produced into various preparations has an excellent anti-depression effect, can be used for avoiding adverse influence of other components in morinda officinalis due to the morida officinalis how polysaccharide extract, and has an unexpected prominent effect in improving sexual dysfunctions caused by medicines.
US20110212049 Polymer compositions of dihydroxyacetone and uses thereof The present disclosure provides injectable synthetic and biodegradable polymeric biomaterials that effectively prevent seroma, a common postoperative complication following ablative and reconstructive surgeries. Provided biomaterials include physically crosslinked hydrogels that are thixotropic, display rapid chain relaxation, are easily extruded through narrow gauge needles, biodegrade into inert products, are well tolerated by soft tissues, and effectively prevent seroma in a radical breast mastectomy animal model.
EP1073429B1 Aerosol formulations of salmeterol xinafoate The present invention relates to formulations comprising particulate products which may be prepared by methods and apparatus using supercritical fluids. More particularly, the invention relates to formulations comprising certain crystalline forms of 4-hydroxy- alpha <1>-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol (salmeterol) 1-hydroxy-2-naphthalenecarboxylate (xinafoate). Accordingly, the present invention provides an aerosol pharmaceutical formulation comprising salmeterol xinafoate with a controlled particle size, shape and morphology, and a fluorocarbon, hydrogen-containing fluorocarbon or hydrogen-containing chlorofluorocarbon propellant.
CA2792035A1 Compositions and methods for treating or preventing immuno-inflammatory disease The present invention relates to compositions and methods for the treatment of immuno-inflammatory conditions comprising the administration of a polyphenolic phytoalexin compartmentalized in a biocompatible and/or biodegradable polymeric carrier, and to the use of biocompatible and/or biodegradable polymeric carriers comprising resveratrol and block copolymers and these compositions with an additional compartmentalized pharmaceutically active agent.
CN101756962A Compound nateglinide valsatan medicinal composition The invention relates to a compound nateglinide valsatan medicinal composition, which is a dual-layer tablet and comprises a first layer of nateglinide and a second layer of valsatan, wherein the first layer is delivered from a self-soluble tablet to be immediately released; and the second layer is released from a self-disintegration or corroded tablet matrix.
DE102006058207A1 New triterpene type compounds comprising a pentacyclic basic structure of nor-oleanan- or non-ursan -types are 11-beta-hydroxysteroid dehydrogenase inhibitors, useful e.g. to treat and prevent the diabetes, depression and glaucoma Triterpene type compounds (I) comprising a pentacyclic basic structure of nor-oleanan- or non-ursan -type, which substantially specifically inhibits a 11-beta -hydroxysteroid dehydrogenase type 1 (11beta -HSD1), are new, where the compound carries a substituent at the position 11C to form hydrogen bond and does not have carboxyl group at the position 20C. An independent claim is included for preparing a specific 11-beta -HSD1 inhibitors from a starting substance, which is a triterpene exhibiting: a pentacyclic basic structure of the oleanan- or ursan-types; a substituent at the position 11C to form hydrogen bond; and a carboxylic acid function, comprising decarboxylating the carboxylic acid function of the starting substance. - ACTIVITY : Antidiabetic; Metabolic; Anorectic; Antilipemic; Antiarteriosclerotic; Nootropic; Antidepressant; Osteopathic; Ophthalmological; Virucide. - MECHANISM OF ACTION : 11beta -HSD1 inhibitor; 1beta -HSD2 inhibitor. The 11beta -HSD1 inhibiting activity of triterpene was tested in Pichia pastoris. The result showed that 30-nor-3beta -hydroxy-11-oxo-18beta -olean-12-en exhibited an inhibition constant (Ki) value of 15 nM.
US20080020992 MULTICISTRONIC CONSTRUCTS WITH siRNA TO INHIBIT TUMORS Multicistronic short interfering RNA constructs targeting in various combinations a human urokinase-type plasminogen activator receptor (uPAR), human urokinase-type plasminogen activator (uPA), human matrix metalloprotease 9 (MMP-9) and cathepsin B (CB) inhibit tumors.
WO2013083040A1 Application of fluoxetine to treatment of depigmentation diseases Disclosed is an application of fluoxetine to treatment of depigmentation diseases, and particularly to treatment of vitiligo and white hair.
EP1948667A2 Thiazolo[4,5-c]pyridine derivatives as mglu5 receptor antagonists The invention relates to compounds of general formula (I) wherein R1, R2 and R3 are as defined in the description as metabotropic glutamate receptor antagonists which are useful in the treatment or prevention of mGluR5 receptor mediated disorders.
US20110262362 Methods for treating obesity The present invention provides methods to reduce or inhibit weight gain by administering inhibitors of the SirT1 protein to a subject. Methods to identify such inhibitors are also disclosed.
US20120148520 Organic Iodine Complex Durable Barrier With Antimicrobial Preparations The present inventions relate to a number of fields including wound healing, a waterless antibacterial disinfectant, a surgical scrub, insect repellant, and methods of treating traumatic injuries, particularly those on the battlefield where there is a need to stabilize the patient and prevent infection.
EP2405921A1 Compositions and methods for silencing apolipoprotein c-iii expression The present invention provides compositions comprising therapeutic nucleic acids such as interfering RNA that target apolipoprotein C-III (APOC3) gene expression, lipid particles comprising one or more (e.g., a cocktail) of the therapeutic nucleic acids, methods of making the lipid particles, and methods of delivering and/or administering the lipid particles (e.g., for the treatment of lipid diseases or disorders such as atherosclerosis or a dyslipidemia such as hypertriglyceridemia or hypercholesterolemia).
WO2013092467A1 7-azaindole inhibitors of crac Disclosed are compounds of Formula (I), useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.
US20100256084 Biological marker for inflammation Inflammatory state in a subject is assayed by determining the level of expression of A3 adenosine receptor (A3AR) in white blood cells (WBC), e.g. circulating WBCs, from the subject. A high level of expression of A3AR is indicative of an inflammatory state in the subject. This assay can be used for determining the severity of inflammation in a subject and monitoring the efficacy of anti-inflammatory treatment. Also, the level of expression may be used for selecting patients to receive an anti-inflammatory treatment that comprises an A3AR agonist.
WO2009002227A1 Rifabutin-based medicinal agent, nanoparticles-containing antimicrobial preparation and a method for the production thereof The invention relates to pharmacology and medicine, in particular to a novel generation of controlled-activity antimicrobial preparations which are based on rifabutin and contain nanoparticles. The inventive method for producing said agent consists in heating the rifabutin, milk and glycol acid copolymer, D-mannitol, polysorbate 80 and dimethylsulphoxide mixture at a determined ratio to a temperature of 50-60°C, in stirring said mixture until a homogeneous transparent liquid is formed and in cooling said liquid to a room temperature. The thus produced suspension, the size of nanoparticles of which is ∼ of 200-400 nm, after having been diluted with water, can be put to good use. Said medicinal agent exhibits broad-spectrum antimicrobial activity and is in practice non-toxic.
US20090111876 Extracts from chlorella This invention relates to an extract of Chlorella sorokiniana, which contains myristic acid, palmitic acid, palmitoleic acid, oleic acid, linoleic acid, linolenic acid, and stearic acid. Also related is use of this extract to treat diabetes, obesity, and dyslipidaemia.
EP2722048A1 Iron bisglycinate chelate for use in treating anaemia The present invention refers to iron bisglycinate chelate for use in oral treatment of anaemia in patients in the preoperative and/or postoperative stage.
WO2005014579A1 Imidazol derivatives of piperdine as histamine antagonists Piperidine compounds according to Formula (I), wherein R1, m, X, n, p, q, Y, Z and Ar are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy and in the preparation of medicaments. The compounds are useful in the treatment of diseases mediated by histamine H3 and H4.
US6943184 For therapy of Alzheimer's disease, Parkinson's disease, Pick's disease, Korsakoff s disease cerebral ageing, of mood disorders, of pain and of tobacco withdrawal A compound selected from those of formula (I): wherein: p represents an integer of from 0 to 6 inclusive, n represents an integer of from 0 to 6 inclusive, R1, and R2 represent a group selected from hydrogen, alkyl, aryl and arylalkyl, or R1+R2 form together with nitrogen carrying them saturated, monocyclic, or bicyclic system, X represents a group selected from oxygen, sulphur, a group —CH═CH—, methylene, a group of formula —HC═N—O— and a group of formula —O—CH2—CH═CH—, in which groups oxygen is linked to Y of the compounds of formula (I), Y represents a group selected from aryl, heteroaryl, arylalkyl, heteroarylalkyl, —C(O)-A, and —C(S)-A, A represents a group selected from alkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, and NR3R4 wherein R3, and R4 represent a group selected from hydrogen, alkyl, aryl, and arylalkyl, or R3+R4 form together with nitrogen carrying them monocyclic, or bicyclic (C3-C10) system, its isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as specific nicotinic ligand of α4β2 receptors.
US20080287464 Depot Formulations Disclosed are formulations and related methods that comprise a non-polymeric, non-water soluble high viscosity liquid carrier material having a viscosity of at least 5,000 cP at 37° C. that does not crystallize neat under ambient or physiological conditions; a specified linear polymer comprising lactide repeat units; and one or more solvents that have a solvent capacity.
US20090209622 Diagnosis of anxiety disorders The invention relates to methods for diagnosing a genetic predisposition or susceptibility for anxiety disorders in a human. The methods include detecting particular markers at the human RGS2 locus in a sample obtained from the human. The invention also relates to the improved diagnosis that is based on the analysis of haplotypes for the RGS2 locus.
CN102000084A Medicine for treating respiratory tract infection The invention belongs to the technical field of medicines and discloses a medicine for treating respiratory tract infection, which is characterized in that active medicinal constituents comprise cefaclor and ambroxol hydrochloride in the weight proportion of (1-6):1. Pharmacological experiments show that the medicine has a favorable effect on treating the respiratory tract infection.
US7052714 Ophthalmic adhesive preparations for percutaneous adsorption Ophthalmic adhesive preparations for percutaneous absorption to be used in treating diseases in the posterior parts of eye characterized by having a drug-containing layer which contains a drug to be delivered to the posterior parts of eye including the crystalline lens, the vitreous body, the uvea and the retina, together with a percutaneous sorbefacient comprising polyoxyethylene oleyl ether and/or isopropyl myristate uniformly dispersed in a base matrix.
CN101875684A Compound with functions of blocking cholesterol esterification and lowering cholesterol The invention relates to a compound, in particular to the compound with the functions of blocking cholesterol esterification and lowering cholesterol. R in the basic structure of the compound represents a new group substituting hydroxyl, comprising -H. -C1, -PO3H3, -NO3, SO4H, -SH, -COOH, -COH, -CH3, -C2H5 and any other groups capable of substituting hydroxyl. In The invention, the compound substituting 3-hydroxyl in a cholesterol structure is used to demonstrate that the new mechanism has a competitive antagonistic effect at the first time in the world; and the action mechanism is to substitute cholesterol 3-hydroxyl, which can competitively interfere absorption of cholesterol in intestinal canal, synthesis in liver and utilization in an issue, thus lowering the low-concentration lipoprotein and the total cholesterol concentration in blood, and having the function of resisting fatty liver and atherosclerosis.
CA2829171A1 Pyrazolidin-3-one derivatives The present invention relates to ethynyl derivatives of formula I wherein X is N or CH; G is N or CH; with the proviso that maximum one of X or G can be nitrogen; R1 is phenyl or pyridyl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; R2 is hydrogen, lower alkyl or may form together with R 4 a C3-C6-cycloalkyl; R3/R3'/R4/R4' are independently from each other hydrogen, lower alkyl or CF3; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
WO2010055082A3 New crystal form of sunitinib malate The present invention relates to novel crystal form of sunitinib malate, to processes for its preparation and to pharmaceutical compositions containing it.
CN101199487A Viramune slice and its preparing method thereof The invention discloses a nevirapine tablet and the related preparation method. The nevirapine tablet is made of 200 portions of nevirapine of 200, 120 to 150 portions of lactose, 50 to 70 portions of microcrystalline cellulose, 15 to 20 portions of sodium carboxy methyl starch, 4 to 5 portions of micronization silica gel, 3 to 4 portions of magnesium stearate and 2 to 3 portions of povidone K30 (based on weight). The invention has the advantages of high finished product rate and low cost.
EP2120907A1 Psychotropic compounds, compositions and methods of use The present invention provides a method for treating or preventing a disease or disorder treatable by the inhibition of serotonin reuptake in a patient, and/or norepinephrine reuptake and/or dopamine reuptake in a patient, the method comprising administering to the patient a neurotransmitter reuptake inhibiting-effective amount of at least one compound of the formula A-L-B (I) or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein A is a psychotropic derivative; L is a linking group comprising two carbon atoms; and B is an alkyl, alkenyl, alkynyl or aralkyl comprising at least one substituent of the formula Q, wherein: the alkyl, alkenyl, alkynyl or aralkyl is optionally substituted with one or more halogens, hydroxyl, cyano, nitro, amino or thiol; and Q is OR6, OC(O)R6, C(O)R6, C(S)R6, CO2R6, C(O)SR6, C(O)NR6R7, C(S)NR6R7, NR6R7, NR6C(O)R7, NR6C(S)R7, NR6C(O)NR7R8, NR6C(S)NR7R8, NR6SO2R7, NR6SO2NR7R8, SR6, SC(O)R6, SC(O)NR6R7, S(O)R6, SO2R6, SO2NR6R7, or NR6SO2NR7R8.
US7465820 Abiotic heparin antagonists The present invention relates to heparin-binding calixarene compounds of general Formula (I) in which R, R1, L and n have the meanings indicated in the description and their use in the biomedical field.
CN103495172A Medicament for treating amphetamine type stimulant dependency and mixed dependency of amphetamine type stimulants and opiates substances The invention discloses a medicament for treating amphetamine type stimulant dependency and mixed dependency of amphetamine type stimulants and opiates substances. The medicament is prepared from the following components by weight percent: 2-95% of antipsychotics, 0.001-5% of alpha2 adrenergic agonists, 0-5% of anticholinergic agent, 0-80% of nonopioid analgesic, and 0-10% of benzodiazepine. The pharmaceutical composition disclosed by the invention achieves an ideal effect when the symptoms of a sufferer abusing stimulants such as benzedrine, or abusing the opiates substances in a merging manner are treated; the withdrawal symptom can be rapidly and obviously controlled; the detoxification recovery rate can be up to over 90%.
CN101904832A Novel application of suramin salt in treating hepatic fibrosis The invention discloses application of suramin salt in preparing medicament resisting hepatic fibrosis. Hepatic fibrosis resistance of the suramin salt is to reduce the content of hydroxyproline in a hepatic tissue, the content of collagenous fiber in the hepatic tissue, the expression level of I and III type collagen mRNA in the hepatic tissue and the serum index of HA, LN, PC III and IV-C4 in hepatic fibrosis. Daily usage for per person of the suramin salt in preparing the medicament resisting hepatic fibrosis is between 9.6 and 38.4mg; and the conventional daily dosage for per people is 10mg, 15mg, 20mg, 28mg, 30mg and 35mg.
WO2012151687A1 Par1 inhibitors for use in the treatment or prevention of paramyxoviridae infections The present invention is concerned with the use of Protease-Activated Receptor-1 (PAR1) inhibitors for preventing or treating a Paramyxoviridae infection in a subject. Described herein are methods, compounds and pharmaceutical compositions useful in addressing such infections, and more particularly infections from human respiratory syncytial virus (hRSV) and human metapneumovirus (hMPV).
EP2658374A1 Hepatoprotectant activity of garcinol The present invention discloses the hepatoprotective potential of garcinol.
CN102370619A Fat-emulsion-emulsified local anesthetic The invention relates to a local anesthetic which is a fat-emulsion-emulsified local anesthetic. According to the invention, the local anesthetic is dissolved in a fat-emulsion, and the solution is a medicine used in local anesthesia such as nerve blocking anesthesia, intraspinal anesthesia, local infiltration anesthesia and local intravenous anesthesia. According to the invention, the fat emulsion and the local anesthetic are processed through heating, oscillating, stirring, homogenizing, and the like, such that the local anesthetic is prepared. With the fat-emulsion-emulsified local anesthetic, original local anesthetic potency is ensured; the toxic reaction limit dose of the local anesthetic is greatly increased, and the severity of happened toxic reaction is reduced. Therefore, patient security is improved. Also, the production process of the medicine is simple, and the price is low.
US20090163491 selective antagonists of A2B adenosine receptors; 6-Chloro-N-[5-(1-cyclopropyl-2,6-dioxo-3-propyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-pyridin-2-yl]-N-(2-pyridin-2-yl-ethyl)-nicotinamide; for treating asthma, diarrhea, insulin resistance, and diabetic retinopathy The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
EP2751109A1 Heterocyclylamines as pi3k inhibitors The present invention provides heterocyclylamine derivatives of Formula (I): wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
CN103232394A Pyrazole-containing compound as well as preparation method and use thereof The invention relates to the field of associated anti-cancer drugs. Specifically, the invention relates to an anti-tumor pyrazole-containing compound with a formula I as well as a preparation method, a medical composition and a use of the compound. The groups are defined in the specification.
US20080260820 Providing effective gastrointestinal tract drug delivery; therapeutic protein having primary amino acid sequence modification Oral dosage formulations of the protease-resistant therapeutic polypeptides are provided. The dosage formulations for administration per dosage per day or per week are higher than the subcutaneous dosage. Included among the oral dosage formulations are tablets and capsules, including enteric-coated forms. Methods for treatment or prevention of diseases or conditions that are treatable or preventable by the administration of such oral dosage formulations of protease-resistant polypeptides are provided.
WO2012110463A1 Active substance for treating inflammatory disease conditions in the oral cavity The invention relates to an active substance, in particular for treating inflammatory disease conditions in the oral cavity, that can be activated by a light source and comprising indocyanine green, wherein a solvent, in particular water, comprises 0.005 - 0.5 mg/ml indocyanine green.
WO2008140064A1 Nutrient composition for prevention and amelioration of lifestyle-related disease Disclosed is a nutrient composition comprising L-arginine, an ω-3 polyhydric unsaturated fatty acid and ribonucleic acid (RNA), and further comprising various minerals including zinc and selenium and various vitamins including vitamins belonging to the groups of vitamin-B and -K which are needed for the activation of the cellular function and a protein syntherized. The nutrient composition enables to aggressively enhance the synthesis and activation of a protein by the action of an energy produced by its lipid metabolism improving activity, thereby preventing and ameliorating a disease such as diabetes, hyperlipemia and fat liver which occurs as a lifestyle-related disease (e.g., a metabolic syndrome).
WO2006132236A1 Mobilizer of leukocyte and/or hematopoietic stem/progenitor cell Disclosed is a mobilize of a leukocyte and/or a hematopoietic stem/progenitor cell which is economically advantageous compared to the administration of a G-CSF preparation and causes reduced adverse side effects. A mobilizer of a leukocyte means an agent for increasing the number of leukocytes, and a mobilizer of a hematopoietic setm/progenitor cell means an agent for mobilizing a hematopoietic stem/progenitor cell from the marrow to the peripheral blood. Particularly, disclosed is a pharmaceutical preparation which is reduced in such adverse side effects (e.g., head ache, fever, bone ache) that may be caused when a G-CSF preparation is administered as a mobilizer of a hematopoietic stem/progenitor cell to the peripheral blood. A pharmaceutical preparation comprising an N-acetylneuraminate sulfate ester or an N-acetylneuraminate homopolymer sulfate ester or a pharmaceutically acceptable salt thereof. When the pharmaceutical preparation is administered, an effect of increasing the number of leukocytes and an effect of mobilizing hematopoietic stem/progenitor cells to the peripheral blood can be observed.
WO2008016913A1 Biologically potent analogues of the dmt-tic pharmacophore and methods of use Disclosed are compounds of formula (I) or pharmaceutically acceptable salts thereof: formula (I) in which R1, R2, and R3 are described herein. Also disclosed is a pharmaceutical composition comprising at least one compound of formula (I) and a pharmaceutically acceptable carrier. Also disclosed is a method of agonizing or antagonizing a µ-opioid or δ-opioid receptor in a mammal in need thereof.
CN103265478A Mercaptonicotinic acid compounds and preparation method thereof The invention belongs to the technical field of medicine, and provides substituted mercaptonicotinic acid compounds and a preparation method thereof. The structural general formula of the compounds is shown as formula I described in the specification, and the compounds comprise a pharmaceutically acceptable salt, ester and solvate. A substituted aniline compound is used as a raw material and reacted with chloroacetyl chloride or bromoacetyl chloride to generate amide, and then the amide is reacted with a mercapto-substituted nicotinic acid or isonicotinic acid compound to obtain the mercaptonicotinic acid compounds. The invention further provides an application of the compounds in a medicament.
US20100130603 Medicament for prophylactic and therapeutic treatment of dermatosis resulting from excessively advanced keratinization A medicament for prophylactic and/or therapeutic treatment of a dermatosis resulting from excessively advanced keratinization, such as non-hereditary inflammatory keratosis and hereditary congenital keratosis, which comprises a substance selected from the group consisting of a cannabinoid agonist and a vanilloid agonist as an active ingredient.
WO2013037482A1 Farnesoid x receptor agonists for cancer treatment and prevention Provided is a Farnesoid X Receptor (FXR) agonist for use in the treatment or prevention of certain cancers, metastases, precancerogenic lesions or angiogenesis in the context of cancer in a patient, wherein the Farnesoid X Receptor (FXR) agonist is administered in a therapeutically effective amount to the patient. Also provided is an FXR agonist for use in inducing NDRG2 gene expression in certain tissues of a patient, wherein the FXR agonist is administered in a therapeutically effective amount to the patient. Also provided is an FXR agonist for use in reducing the rate of proliferation, migration, metastasis or angiogenesis of certain tumors.
CN102670864A Medicine composition with antioxidant function for treating cardiovascular and cerebrovascular diseases and sugar diabetes The invention relates to a medicine composition with the antioxidant function for treating the cardiovascular and cerebrovascular diseases and the sugar diabetes, and relates to the technical field of medicines. Through aiming at the causes of the cardiovascular and cerebrovascular diseases and the sugar diabetes, combining the advantages and disadvantages of various medicines for treating the cardiovascular and cerebrovascular diseases and the sugar diabetes at present, and adopting a compound technique, grape seed extracts, ginkgo biloba extracts, chitosan oligosaccharide and chitosan are effectively combined together. The invention provides the medicine composition with a strong antioxidant effect for treating the cardiovascular and cerebrovascular diseases and the sugar diabetes at the same time.
WO2011117798A1 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9h-carbazole derivatives and their use as prostaglandin d2 receptor modulators The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I), wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
CN101269021A Puerarin sustained-release dropping pills and preparation method thereof The invention discloses a medicine used for curing the diseases such as coronary heart disease, angina, miocardial infarction, retinal artery or vein occlusion and sudden deafness, etc. and a preparation method thereof. The invention aims at making up the deficiency of the prior art and provides a puerarin sustained-release pill preparation. In the constituents adopted by the prior art, the puerarin sustained-release pill related by the invention utilizes hydrophilic framework material and hydrophobic framework material as stroma and is added with stabilizing agent vitamin C, so as to effectively overcome the defects of the prior art and ensure that the medicaments do not have apparent change relating to the material contents within the valid storing period; furthermore, the puerarin sustained-release pill has the advantages of enough medicine release, controllable medicine releasing time, few times needed by the patient to take the medicine, long time for taking effect and high bioavailability, and is suitable for clinic and family.
CN103169720A Application of anthracene nucleus antibiotic and its pharmaceutical salt for treating retinal vein occlusion The invention discloses an application of anthracene nucleus antibiotic and its pharmaceutical salt for treating retinal vein occlusion. The invention found that the anthracene nucleus antibiotic and its pharmaceutical salt have good effect on treatment of retinal vein occlusion, and especially the anthracene nucleus antibiotics can be prepared to prolonged action preparations such as a nano preparation, a microballoon preparation, liposome and hydrogel, the toxicity of anthracene nucleus antibiotic is reduced, and the anthracene nucleus antibiotic enables ophthalmic administration, administration dosage is simultaneously enlarged, the duration time of drug effect is long, the medicament curative effect is stronger than that of the common preparations of the anthracene nucleus antibiotic, when the ophthalmic administration is carried out, the anthracene nucleus antibiotic has good treatment effect for treating retinal vein occlusion, and the blank that no medicine is good for treating retinal vein occlusion can be filled.
CN102532192A Acetaminophen-cyclophosphamide anti-tumor drug and preparation method thereof The invention provides a chlormethine compound with double activity function groups and application of the chlormethine compound serving as an anti-tumor drug. A structure of the compound is described as follows. In-vitro anti-tumor experiments prove that the compound has good inhibiting effect on liver cancer cells of the human body. In-vitro deoxyribose nucleic acid (DNA) crosslinking experiments prove that the compound has good crosslinking effects on plasmid DNA. Mouse analgesia experiments prove that the compound has good analgesia effects. The chlormethine compound is simple in synthesizing steps and good in anti-tumor effects, possibly simulates the analgesia effects of acetaminophen in vivo, is an anti-tumor drug with double functions, and has great medical value.
US20110206631 Ion binding polymers and uses thereof The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising potassium binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hyperkalemia, such as hyperkalemia caused by renal failure and/or the use of hyperkalemia causing drugs.
US20110105587 Target sequences and methods to identify the same, useful in treatment of neurodegenerative diseases The present invention relates to methods and assays for identifying agents capable of inhibiting the mutant huntingtin protein, inhibiting or reducing cell death, in particular cell death associated with polyglutamine-induced protein aggregation, which inhibition is useful in the prevention, amelioration and/or treatment of neurodegenerative diseases, and Huntington's disease more generally. In particular, the present invention provides methods and assays for identifying agents for use in the prevention and/or treatment of Huntingtons disease. The invention provides polypeptide and nucleic acid TARGETs and siRNA sequences based on these TARGETS.
US7081261 Crystal structure, enzyme resistance, nonhydrolyzing, nonabsorption in the small intestine, and passes into the large intestine, fermentation by colonic microflora to maintain colonic health This patent pertains to a resistant starch prepared by fully debranching a low amylose starch using isoamylase. Such resistant starch is useful in edible products, including nutritional supplements.
EP1685131B1 Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones The present invention provides a compound of the formula (I) where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. The present invention also provides methods for using compounds of Formula (I) in treating p38 mediated disorders in a patient.
WO2012046772A1 Prophylactic and/or therapeutic agent against lymphedema Provided is a new prophylactic and/or therapeutic agent against lymphedema, for which until now there has been no effective means of treatment. The prophylactic and/or therapeutic agent against lymphedema contains, as an active ingredient, a compound represented by formula (1) (in the formula, R1 represents an organic radical, X represents -CH2CH2- or -CH=CH-, and R2 represents a hydrogen atom or alkyl radical), a lactone derivative thereof, or a salt of the compound or the lactone derivative.
WO2011045267A1 Polymorphs of pardoprunox This invention relates to a novel process for the preparation of 7-(4-methyl-1 -piperazinyl)benzoxazol-2(3H)-one hydrochloride, a partial dopamine-D2 receptor agonist and a full serotonin 5-HT1A receptor agonist. Formula (I) 7-(4-methyl-1-piperazinyl)benzoxazol-2(3H)-one hydrochloride The invention also relates to polymorphic forms of said compound, as well as to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in affections or diseases of the central nervous system, caused by disturbances of the dopaminergic and/or serotonergic systems, for example: anxiety disorders (including generalised anxiety, panic disorder and obsessive compulsive disorder), depression, autism, schizophrenia, Parkinson's disease, restless leg syndrome, disturbances of cognition and memory.
WO2006074057A3 Pyrimidine derivatives as kinase modulators and method of use The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a farmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O-R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14. C(O)O-C1-C6 alkyl, or N(R13)-C(O)-C1-C6 alkyl; Y is H, halo, OH, C1-C6 alkyl, C0-C6 alkyl-NR,15R16, NRI5R,6, C1-C6 alkoxy, -N(R13)-(CH2)n-NR15R16, -C(O)O-C1-C6 alkyl, -O-(CH2)n-NR15R16, -C(O)-C1-C6 alkyl, -C0-C6-alkyl-R21, -O-R21, -C(O)-R21, -O-(CH2)n-R21, -C(O)-NR13R14, -C(O)-N(R13)-aryl, -C(O)-N(R13)(CH2)n-NR15R16, -C(O)-N(R13)-(CH2)n-aryl -C(O)-N(R13)-(CH2)n-heterocyclyl; or X and Y together with the atoms to which they are attached form a 4-7 membered heterocyclyl or heteroaryl group containing one or two heteroatoms independently selected from O, N, and S. Z is H, NR2R3, -S-R2a, or -0-R2a
CA2349168C Hyaluronic acid gel, method of its production and medical material containing it A gel made of hyaluronic acid alone which is hardly soluble in a neutral aqueous solution and has fluidity enough to be easily ejectable from an injector
WO2013060881A1 Pyridopyrimidines and their therapeutic use A compound of formula (I) Wherein at least one of X and Y is N and the other of X or Y is either N or CR2. Such compounds may be useful in the therapy of inflammatory disorders, allergic disorders, dermatological disorders, autoimmune disease, lymphatic disorders, and immunodeficiency disorders.
CA2209775C Analogues of n-acetylardeemin, method of preparation and uses thereof The present invention provides a compound having structure (I) wherein R1, R6 and R7 are independently hydrogen, OH, NH2. SH, halogen, C1-C9 linear or branched chain alkyl, alkylmercapto, alkylamino, dialkylamino, alkoxy, phenyl, etc; wherein R0 and R2 are independently hydrogen, OH, linear or branched chain alkyl, -CR3R3-CH(O)CH2, -CR3R3-CH2CH3, -CR3R3-CH2CH2OH, -CR3R3-CH(OH)R4 or -CR3R3-CH-CHR4, wherein R3 and R4 are independently hydrogen, halogen, C1-C9 linear or branched chain alkyl, phenyl, etc; wherein R5 is hydrogen, C1-C9 linear or branched chain alkyl, phenyl, etc; an wherein R8 is hydrogen C1-C9 linear or branched chain acyl, benzoyl, etc; with the proviso that (a) when R2 is -CR3R3-CH(O)CH2, -CR3R3-CH2CH3, -CR3R3-CH2CH2OH, -CR3R3-CH(OH)R4 or -CR3R3-CH=CHR4, then R0 is hydrogen;(b) when R0 is -CR3R3-CH(O)CH2, -CR3R3-CH2CH3, -CR3R3-CH2CH2OH, -CR3R3-CH(OH)R4 or -CR3R3-CH=CHR4, then R2 is OH;and (c) when (i) R0 or R2 is -CR3R3-CH=CHR4, (ii) R3 and R5 are CH3 and (iii) R4 is hydrogen, then R1, R6 and R7 are not all hydrogen.Also provided are related compounds and compositions, and methods of inhibiting the growth of multidrug resistant cells by means of MDR reversal, collateral sensitivity and quantitative synergism.
WO2010055894A1 Organic arsenic-containing compound, and composition for inhibiting growth of tumor comprising the compound Disclosed is a novel anti-tumor compound. Also disclosed is a composition comprising the compound. Specifically disclosed is a composition for inhibiting the growth of a tumor, which comprises a purified and isolated organic arsenic-containing compound. The organic arsenic-containing compound is an arsenic-bound lipoprotein. The arsenic-bound lipoprotein comprises a phospholipid, arsenic, and a peptide composed of at least four amino acid residues and has the following physical properties: the lipoprotein has the form of milky white crystals; the lipoprotein is soluble in water, methanol and 70% ethanol, but is insoluble in ethanol; the lipoprotein turns purple-blue when it reacts with a ninhydrin reagent; the lipoprotein has an Rf value of 0.18±0.02 in the thin-layer chromatography using a developing solvent composed of n-butanol, glacial acetic acid, ethanol and water (4:1:1.5:2); and the lipoprotein has a molecular weight of 5000 or less.
US20130028992 Herbal-Based Solution for Treating Symptoms of Nasal Conditions An herbal-based solution includes a first amount of wasabi comprising at least an allyl isothiocyanate component, and a second amount of saline solution. The saline solution and the organic material are combined to substantially dilute the wasabi in the saline solution to produce the herbal-based solution. The herbal-based solution further has anti-inflammatory, anti-microbial and anti-coagulative properties. The wasabi may include Eutrema Wasabi. The herbal-based solution is deliverable as a nasal.
US8163701 Prodrugs of active agents Disclosed herein are prodrugs of active agents which contain at least one amine, phenol, carboxylic acid, or thiol functionality. Also disclosed herein are methods of making prodrugs of active agents, pharmaceutical compositions of prodrugs of active agents and methods of using prodrugs of active agents and pharmaceutical compositions.
WO2010056216A1 Pharmaceutical composition comprising ibuprofen, pseudoephedrine and chlorpheniramine The present invention relates to a pharmaceutical composition comprising ibuprofen as the active agent, preferably chloropheniramine maleate as an antihistaminic agent, preferably pseudoephedrine HCl as a sympathomimetic amine, and an alkaline salt, such as sodium bicarbonate, in an amount adequate to maintain the final solution's pH level between 7 and 9.
CN102319208A Suspension composition for treating oral mucositis caused by chemoradiotherapy The present invention discloses a suspension composition for treating oral mucositis caused by chemoradiotherapy, and relates to a new drug for treating oral mucositis. The suspension composition comprises: 1, local anesthetics; 2, histamine 1 receptor antagonists; 3, a mucosal repairing agent and a drug dispersing agent; 4, an anti-foaming agent; 5, microcrystalline cellulose; 6, unreactive assistant materials; 7, pure water. The preparation method comprises: 1, preparing a solution I; 2, preparing a solution II; 3, adding the solution I to the solution II at a stirring state, completely stirring, adjusting the pH value of the mixed solution to 6-9 to obtain the suspension composition. According to the present invention, the suspension composition provided by the present invention has characteristics of good uniformity and strong stability, is not easy to agglomerate when the suspension composition is placed for a long time; the preparation method has characteristics of simple process and low production cost; the suspension composition can be applicable for treating the oral mucositis caused by the chemoradiotherapy, and severe mouth ulcers caused by anaerobic bacteria; the suspension composition provides effects of analgesia, inflammation eliminating and mucosa repairing; the clinical efficacy of the suspension composition is obvious; the use of the suspension composition is convenient and safe.
CN102988987A Pharmaceutical composition for treating hyperproliferative skin disease and preparation of pharmaceutical composition The invention belongs to the field of pharmacy and particularly relates to a pharmaceutical composition for treating hyperproliferative skin disease and a preparation of the pharmaceutical composition. The pharmaceutical composition comprises the following components by weight percent: 0.001-0.01% (W/W) of calcipotriene, 0.05-2% (W/W) of tazarotene and 0.05-2% (W/W) of adrenocortical hormone.
US20080069886 Spironolactone nanoparticles, compositions and methods related thereto This invention relates to nanoparticles comprising spironolactone. The nanoparticles have a mean diameter, measured by photon spectroscopy, in the range of from about 300 nm to about 900 nm.
WO2008061373A1 Combination treatments for alzheimer's disease and similar diseases The invention relates generally to novel compositions and methods comprising a cyclohexanehexol and a secretase inhibitor The compositions and methods provide beneficial effects, in particular sustained beneficial effects, in the treatment of diseases involving a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence, such as Alzheimer's disease and related neurodegenerative disorders.
US20080026984 Methods for treating inflammatory disease by administering aldehydes and derivatives thereof A method is disclosed for treating inflammatory disease in an animal in need thereof by administering to the animal a pharmaceutical composition containing an anti-inflammatory effective amount of an organic aldehyde compound or a derivative thereof in a pharmaceutically acceptable vehicle.
WO2008024438A3 2-phenoxy pyrimidinone analogues 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
US7427416 Methods of treating conditions using metal-containing materials Methods of treating conditions using metal-containing materials are disclosed. Exemplary conditions include bacterial conditions, biofilm conditions, microbial conditions, inflammatory conditions, fungal conditions, viral conditions, autoimmune conditions, idiopathic conditions, hyperproliferative conditions, noncancerous growths, cancerous conditions and combinations of such conditions. In certain embodiments, the metal-containing material is an atomically disordered, nanocrystalline silver-containing material.
US20110179502 Modulation of gm98 (mrf) in remyelination The present invention provides compositions and methods for regulating remyelination and promoting oligodendrocyte differentiation by modulating GM98 (also known as MRF) expression and activity. Compositions and methods for treating neuropathies and screening for bioactive agents are also provided herein.
CN101214244B Antibiotic medicament containing amoxicillin nano granule and potassium clavulanate The present invention discloses an antibiotic medicine which contains amoxicillin nano-particles and clavulanate potassium and is made from 0.2 percent to 0.4 percent of amoxicillin, 0.02 percent to 0.25 percent of the clavulanate potassium, 0.5 percent to 2 percent of carrier, 0.5 percent to 2 percent of stabilizing agent, 0.5 percent to 2 percent of surfactant and 93 percent to 98.5 percent of distilled water according to the following method that: carrier monomers and the surfactant are dissolved in the distilled water completely; the amoxicillin is added; pH value is adjusted to be 2 to 3; butyl cyanoacrylate is added while being stirred by magnetic force and is stirred continuously for 5 to 12 hours, the pH value is adjusted to be 6 to 7, flaxen amoxicillin poly butyl cyanoacrylate nano-particle colloid solution is obtained; the clavulanate potassium is added by the proportion of the amoxicillin and the clavulanate potassium of 2:1 to 10:1 to obtain the antibiotic medicine which not only has simple preparation method but also has the advantages of wide spectrum, high efficiency, being targeted, slow-released, safe, etc.
EP1827464A1 Zinc-based compositions and methods of use The invention relates generally to zinc-based compositions for topical use in humans and animals, and methods therefor. The invention further relates to the use of zinc-based compositions in wound treatment, cleaning and other therapeutic applications.
US20070259908 Mitochondria Activators The present invention provides a mitochondrial activator containing pyrroloquinoline quinone, preferably pyrroloquinoline quinone and coenzyme Q (particularly reduced coenzyme Q) as active ingredients. In addition, the present invention provides a mitochondrial activator containing citric acid, preferably citric acid and coenzyme Q (particularly reduced coenzyme Q), as active ingredients. Since pyrroloquinoline quinone or citric acid exhibits a synergistic mitochondria activating effect with coenzyme Q (particularly reduced coenzyme Q), a high effect can be obtained even at a low dose. According to the present invention, therefore, a safer and practical mitochondrial activator is provided. The present invention further provides an agent for the prophylaxis or treatment of a disease caused by mitochondrial dysfunction.
US20080194682 administering inhibitors of endopeptidase such as thiorphan or candoxatril, to effect bone elongation; achondroplasia The present invention discloses pharmaceutical compositions for the treatment of skeletal dysplasias, comprising as an active ingredient at least one natriuretic peptide. Unexpectedly, it has been shown that the natriuretic factors may be effective for bone elongation in situations of abnormal bone growth especially for achondroplasia. The effects of the natriuretic peptide may be further enhanced by prolonging its residence time or action at the target site.
US20080070899 (Calcitonin gene related peptide); headache, migraine and cluster headache; spiropiperidine-substituted azepan-2-ones such as 1-(2,2,2-trifluoroethyl)-3-(1-oxo-2,8-diazaspiro[4.5]decan-8-yl-aminocarbonylamino)6-(2,3-difluorophenyl)azepan-2-one The present invention is directed to compounds of Formula I: Formula I: I and Formula II: (where variables R1, R2, R3, R4, A, B, J, Q, T, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
CN1613448A Oral disintegrated and/or oral soluble solid hydrocyclo-benzenenonate An oral disinfecting and/or dissolving medicine of phenylcycloononyl ester hydrochloride for treating motion sickness contains methyl acrylic acid polymer or cyclodextrin and its derivative, such as beta-cyclodextrin. Its advantage is short oral disintegrating and/or dissolving time (1-30 S).
WO2014073740A1 Anti-cancer drug and treatment method for treating tumors having multidrug resistance The present invention provides an anti-tumor drug comprising, as active ingredients, Wip1 inhibitors and Mdm-2/p53 interaction inhibitors so as to effectively treat malignant tumors.
CN101780048A Enteric solid preparation using pantoprazole sodium as major ingredients and preparation method thereof The invention provides an enteric solid preparation using pantoprazole sodium as major ingredients and a preparation method thereof. The invention relates to an enteric solid preparation using pantoprazole sodium or hydrate thereof as active ingredients and a preparation method thereof. The invention aims at providing a novel pantoprazole sodium preparation for a large number of patients and medical personnel, and the novel pantoprazole sodium preparation fully exerts the medicine curative effect, reduces the adverse effect, is convenient for children and old people to take in a decrement way, is convenient to carry, store and transport, and is suitable for large-scale production. The invention uses the pantoprazole sodium or the hydrate thereof as the active ingredients, some accessory ingredients of specified types are proportionally added into the ingredients for being prepared into enteric grains or micropills according to the process provided by the invention, and the ingredients can be further prepared into dry suspension preparations or capsules.
CN1969848A Externally applied ointment for treating impetigo The invention discloses an external ointment to treat impetigo, which is characterized by the following: adopting vanishing cream, alficetin, chlorpheniramine and vitamin C as raw material; grinding alficetin, chlorpheniramine and vitamin C to blend together; adding vanishing cream to synthesize lacte ointment on the injury; sealing; reserving at dark and cool place.
WO2007138905A1 Intestinal eosinophil-suppressing composition To promote the growth of human beings or animals, prevent the onset of diarrhea and prevent or ameliorate various diseases, it is intended to provide a substance which has an effect of decreasing eosinophils in the intestinal tract and a feed containing the same as a feed additive. Namely, an intestinal eosionphil-suppressing composition which contains an α-linked galactooligosaccharide as the active ingredient. When added in an amount of from 0.01 to 10% by weight, in terms of the saccharide, to an animal feed, this composition is useful in providing an intestinal eosinophil-suppressing feed.
WO2005010189A1 OLIGONUCLEOTIDE INHIBITING THE EXPRESSION OF StAR-BINDING PROTEIN (SBP) GENE AND METHOD THEREFOR A means of inhibiting the production of an StAR-binding protein which binds to StAR protein serving as a cholesterol transportation promoter and thus controls the function of the StAR protein. By damaging its function, apoptosis is introduced specifically to a cancer cell. A protein interacting with StAR protein is found out. Then an RNA fragment homologous with a gene sequence specific to this StAR-binding protein (SBP) is synthesized and introduced into a cancer cell. As a result, it is confirmed that the expression of the StAR-binding protein is thus inhibited and, furthermore, the appearance of an apoptotic cell is confirmed.
WO2008067756A1 3-pyrrolo-cyclohexylene-2-dihydro-indolinone derivatives and uses thereof 3-pyrrolo-cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay show that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.
WO2010117090A1 Novel isoquinolinyloxymethyl heteroaryl derivatives The present invention relates to a compound represented by a formula (I): wherein: X1 to X5 are all CR and the like, and a formula (II): is a pyridinyl group, a pyrrolyl group and the like, X is N(R2), an oxygen atom or CH2, Y is a lower alkylene group, R is a hydrogen atom, a halogen atom and the like, R1 is a halogen atom, a cyano group and the like, R2 is a hydrogen atom or a lower alkyl group, m is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof.
WO2013067084A1 Silylated azulenyl nitrone spin traps as chromotropic superoxide detectors Silylated nitrones and methods of detecting and/or superoxide using silylated nitrones are disclosed herein.
CN102643272A Novel thieno [3, 2-d] pyrimidine compound The invention relates to a thieno [3, 2-d] pyrimidine compound shown in the formula I, a stereomer thereof and a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, wherein substituent groups R1 and R2 have the meanings given in the specification. The invention also relates to the usage of the compound shown in the formula I in preparing drugs for treating and/or preventing cancer and other poliferative diseases.
CN101407502B N-(t-butoxy carbonyl ) timonacic compounds, and preparation and use thereof The invention relates to a class of N-(tert-butoxycarbonyl) timonacic compounds of the right general formula, and the novel N-(tert-butoxycarbonyl) timonacic compounds can inhibit not only Gram positive bacterial strains but also Gram negative bacterial strains, and the result also shows that one of the compounds has strong capability of inhibiting pseudomonas aeruginosa strains and great potential in becoming a class of thiazolidine antibacterial drugs. The invention discloses a manufacturing method of the compounds.
WO2011068546A3 Prognosis, diagnosis and identification of multiple myeloma based on global gene expression profiling The present invention provides a diagnostic or prognostic indicator of multiple myeloma that comprises a global expression profile of total miRNA in the subject with a pattern of 39 up-regulated and 1 down-regulated gene as listed in Table 1. Also provided are methods of diagnosing multiple myleoma in a subject and determining prognosis of a subject with multiple myeloma by demonstrating the subject shows the expression profile of the diagnostic or prognostic indicator and further calculating a risk score and/or a proliferation level based on a group of 70 genes and 11 genes, respectively, such that high scores and levels concomitant with the miRNA expression profile correlates to a diagnosis and/or a poor prognosis. In addition, methods of treating multiple myeloma with a therapeutic inhibitor of an miRNA maturation pathway in the subject and for screening for therapeutic inhibitors that inhibit AGO2 and/or DICER1 genes are provided.
WO2010067010A3 Derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics The invention relates to derivatives of morphine-6-glucuronide having formula (I) wherein R1 is a 5-membered heteroaromatic group optionally substituted by one or more substituents selected from among halogen atoms and (C1-C4)alkyl, halogen, hydroxyl, halo(C1-C4)alkyl, halo(C1-C4)alkyloxy, (C1-C4)alkyloxy, aryl(C1-C4)alkyl and aryl groups, said aryl group being optionally substituted by one or more groups selected from among (C1-C4)alkyl, halo(C1-C4)alkyl, hydroxyl and (C1-C4)alkyloxy groups, in the form of a base or acid addition salt, as well as in hydrate or solvate form. The invention also relates to the preparation method thereof and to the use of same in therapeutics.
EP1699792A1 Piperazine, 1,4¨diazepane, 1,4¨diazocane, and 1,5¨diazocane fused imidazo ring compounds Piperazine, [1,4]diazepane, [1,4]diazocane, and [1,5]diazocane fused imidazo ring compounds (i.e., imidazoquinolines, tetrahydroimidazoquinolines, imidazonaphthyridines, tetrahydroimidazonaphthyridines, and imidazopyridines), pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
CN103356583A Application of Sarcaboside A in preparing anti-platelet aggregation medicine The invention relates to an application of Sarcaboside A in preparing an anti-platelet aggregation medicine. The application of the Sarcaboside A in preparing an anti-platelet aggregation medicine is disclosed for the first time; since a brand new skeleton type is adopted and the anti-platelet aggregation activity thereof is unexpectedly high, the possibility of other compounds giving any prompt is avoided, and the Sarcaboside A has outstanding substantive features; and a remarkable progress is made in applying the Sarcaboside A to the platelet aggregation resistance.
WO2014005150A1 Crystalline forms of l-(2-((lr,3s,5r)-3-( (2 -fluoro-3 - (trifluoromethoxy) phenyl) carbamoyl) - 2 -azabicycl o [3.1.0] hexan- 2 -yl) - 2 -oxoethyl) - 5 -methyl - 1h - pyrazolo [3, 4 -c] pyridine - 3 - carboxami de and salts thereof Crystalline forms and pharmaceutically acceptable salts of l-(2- ((1 R,3S,5R)-3-((2-fluoro- 3-(trifluoromethoxy)phenyl)carbamoyl)-2- azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-5- methyl-1 H-pyrazolo[3,4- c]pyridine-3-carboxamide. l-(2-((l R,3S,5R)3-((2-fluoro-3- (trifluoromethoxy)phenyl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl) -2-oxoethyl)-5- methyl-1 H-pyrazolo[3,4-c]pyridine-3-carboxamide is useful in treating Age-related Macular Degeneration (AMD).
US20060229239 Novel curcuminoid-factor VIIa constructs as suppressors of tumor growth and angiogenesis The fluorinated curcuminoid (3,5-bis-(2-fluorobenzylidene)-piperidin-4-one-acetate is about ten times more effective at arresting the growth of tumor cells than cisplatin. The present invention provides methods to deliver a cytotoxic compound, such as a curcuminoid, specifically to cancer cells and to the vascular endothelial cells that nourish solid tumors. The method involves tethering the drug to a protein such as in factor VIIa that retains high affinity for the surface protein tissue factor. Upon complexation, the resulting heterodimer is endocytosed and the drug is subsequently liberated inside the target cell via proteolytic cleavage. The present invention further provides for the synthesis of novel curcuminoid-tether-linker-factor VIIa compositions and for methods of delivery of effective doses of the novel compositions to target tumor or endothelial cells in a patient
WO2005074988A1 Nerve cell differentiation inducer It is intended to provide a nerve cell differentiation inducer containing a synoviolin expression inhibitor which is a drug useful in treating nerve diseases, in particular, Alzheimer’s disease, Parkinson’s disease, peripheral nerve injury or spinal injury. Examples of the synoviolin expression inhibitor include siRNA or shRNA to a gene (SEQ ID NO:1 or 2) encoding synoviolin, a decoy nucleic acid binding to the transcriptional factor of a synoviolin gene promoter to thereby inhibit the activity of the promoter, and an antisense oligonucleotide to a gene encoding synoviolin. This nerve cell differentiation inducer is useable in treating nerve system diseases such as Alzheimer’s disease, Parkinson’s disease, peripheral nerve injury and spinal injury.
US7265136 Substituted stilbene compounds with vascular damaging activity A compound for use in inducing necrosis in vascular tissue of a tumor in an animal. The compound contains a first moiety which is a cis-stilbene moiety and a second moiety which is an inhibitor of the formation or action of nitric acid. Also, a method for inducing necrosis in vasculature of a tumor in an animal by administering to the animal the compound in an amount effective for inducing the necrosis.
EP1458447B1 Combination of cytochome p 450 dependent protease inhibitors The present invention relates to a method for improving the pharmacokinetics of hexahydrofuro[2,3-b]furanyl containing HIV protease inhibitors comprising administering to a human in need thereof a combination of a therapeutically effective amount of a hexahydrofuro[2,3-b]furanyl containing HIV protease inhibitor, and a therapeutically effective amount of a cytochrom P450 inhibitor.
CN103288881A Dual-core organic metal ruthenium compound with anti-tumor activity The invention discloses a dual-core organic metal ruthenium compound with anti-tumor activity. The chemical name of the dual-core organic metal ruthenium compound is bis-hexafluorophosphate phenylacetaldehyde dibenzene-N4-methyl-thiosemicarbazide dimethyl isopropyl benzene ruthenium (II). A preparation method of the dual-core organic metal ruthenium compound comprises the following steps of: 1) preparing a product A; 2) preparing phenylacetaldehyde benzene-N4-methyl-thiosemicarbazide; 3) dissolving the phenylacetaldehyde benzene-N4-methyl-thiosemicarbazide (19mg, 0.1mmol) and the product A (32mg, 0.05mmol) into 6ml of acetone, stirring at normal temperature for 12 hours, to form red transparent solution, then adding 16.3mg (0.1mmol) ammonium hexafluorophosphate, capping a bottle cap, standing for 12 hours to have a great deal of particulate red crystals, namely products. Proved by the in-vitro anti-tumor experiments, the dual-core organic metal ruthenium compound has obvious inhibition effect on liver cancer BEL7404 tumor cell strains.
CN101830961B Ursolic acid ester derivatives, preparation method thereof and application thereof The invention discloses ursolic acid ester derivatives, namely ursolic acid 4-[1-acetyl-3-substituted phenyl-4,5-dihydro-2- pyrazoline-5-yl] phenol ester and ursolic acid 4'-substituent-4-chalcone ester. The structural formulas are as below, wherein R is hydrogen or methyl or methoxyl or halogen. Part compounds are stronger than ursolic acid in anti-tumor activity. The preparation method of the ursolic acid ester derivatives comprises the following steps: (1), synthesizing 4'-substituent-4-hydroxy chalcone; (2), synthesizing 4-(1-acetyl-3-substituted phenyl-4,5-dihydro-2-pyrazollin-5-yl)phenol; and (3), synthesizing the ursolic acid 4-[1-acetyl-3-substituted phenyl-4,5-dihydro-5-yl] phenol ester and the ursolic acid 4'-substituent 4-chalcone ester.
US8580783 [1,2,4]triazolo [1,5-c]pyrimidine derivatives as Hsp90 modulators The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
US20110060011 Oxazole compounds compositions and methods of use The present invention relates generally to compounds represented in Formula (I), pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.
EP1560582A2 AZAINDOLE DERIVATIVES AS INHIBITORS OF p38 KINASE The invention is directed to methods to inhibit p38 kinase, preferably p38-α using compounds which are azaindoles wherein the azaindoles are coupled through a piperidine or piperazine type linker to another cyclic moiety.
EP2090301A1 3-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-1-propanon und its use in cosmetic and pharmaceutical preparations Cosmetic or pharmaceutical preparation comprises: (a) an antiinflammatory active agent comprising 3-(4-hydroxy-3-methoxy-pheny l)-1-(4-hydroxy-phenyl)-propan-1-one (I); (b) >= 1-4 antiinflammatory active compound; and one or more components (a) and (b) compatible with cosmetic and/or pharmaceutical base material, auxiliary material or additives. An independent claim is included for the 3-(4-hydroxy-3-methoxy-pheny l)-1-(4-hydroxy-phenyl)-propan-1-one (I) useful as a drug. - ACTIVITY : Antiinflammatory; Dermatological; Antiallergic. - MECHANISM OF ACTION : None given.
CN101717359A Method for synthesizing indapamide The invention discloses a method for preparing indapamide from chloro-1,3-dimethyl-2-climiqualine as a condensing agent, comprising the following concrete steps of: under the action of a condensing agent of chloro-1,3-dimethyl-2-climiqualine and organic base, reacting 4-chloro-3-sulfamoylbenzoic acid with N-amido-2-methylene indoline or corresponding salts thereof in inert solvent at room temperature and carrying out purification treatment to obtain a target product of the indapamide, wherein the corresponding salts of the 4-chloro-3-sulfamoylbenzoic acid and the N-amido-2-methylene indoline are hydrochloride, hydrobromide, mesylate or paraaminomethyl benzene sulfonate. The invention has the advantages of high yield in the technological process, low cost and simple and convenient operation, and can meet the requirement of large-scale production.
CN103408606A N-(2-deoxy-lactose-2-group)-3-(substituted phenyl) acrylamide and medical application thereof The invention relates to the field of medicinal chemistry and particularly relates to a class of N-[1, 3, 6-tri-O-acetyl-4-O-(2, 3, 4, 6-quadri-O-acetyl)-beta-D-galactosyl]-2-deoxy-beta-D-glucosyl group]-3-(substituted phenyl) acrylamide (I), as well as a preparation method and an application thereof in restriction of vascular endothelial cell proliferation and chick embryo chorioallantoic membrane neovascularization.
US8337877 Reduction of infection associated with medical device Anti-infective articles capable of preventing infection associated with implantation of medical devices include low levels of anti-infective agents, may cover only a fraction of the portion of the medical device and be effective, or may rapidly elute anti-infective agent, without sustained elution, and still be effective.
CN101822653A Clindamycin phosphate film agent and preparation method thereof The invention discloses a clindamycin phosphate film agent, which is mainly prepared by the clindamycin phosphate which comprises the following components based on parts by weight: 1-100 part of clindamycin and 5-500 parts of film-forming material. The agent is directly used on the infection part, and has high concentration of local medicine, fast efficiency, low dosage and no adverse reaction.
EP2701709A1 Method for modulating ion transporter The present invention relates to a method for modulating ion transporter or treating disturbances of electrolyte transport during disease state, comprising an administration of a fatty acid derivative to a mammalian subject. The present invention also relates to a composition for modulating ion transporter or treating disturbances of electrolyte transport during disease state, comprising a fatty acid derivative.
US20130052172 Methods for diagnosing and treating cardiac defects The present disclosure defines a method for identifying and/or treating risk and/or occurrence of cardiac defect. As is shown herein, microbiomes are reproducibly and detectably associated with cardiac defect risk factors and changes to the microbiome can directly alter cardiac defect risk. The present disclosure demonstrates that microbial signatures can be used to characterize components of microbiomes that associate with altered risk or occurrence of cardiac defects and to identify treatments to reduce risk or severity of cardiac defects.
WO2011151434A1 Novel compounds, pharmaceutical composition and methods for use in treating metabolic disorders The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.
WO2005120572A1 Photodynamic therapy for the treatment of hyperactive sebaceous gland disorders using topically applied hydrophobic green porphyrins The present method involves the photodynamic treatment of hyperactive gland disorders. The method involves the topical administration of a photosensitizer composition comprising hydrophobic and/or lipophilic green porphyrins such as lemuteporfin, polyethylene glycol and skin penetration enhancers such as oleyl alcohol and TRANSCUTOLTM to affected skin and subsequent exposure of that skin to energy of a wavelength capable of activating the photosensitizer.
EP1455805B1 A process for obtaining a zinc oxide containing product for skin-healing, care and protection in children and adults The procedure for obtaining a product for skin-healing, care and protection in children and adults consists thereto that a zinc oxyde powder in quantity of 0.4 gr and talcum powder in quantity of 0.6 gr are dissolved in 1 gr of paraffin oil in duration of 1-2 minutes until completely homogenized. Lanolin in quantity of 27 gr, Vaseline in quantity of 23 gr, paraffin oil in quantity of 11 gr, distilled water in quantity of 10 gr, boric acid powder in quantity of 4 gr and almond water in quantity of 8 gr are put in a paten where they are melted in water bath at the temperature of approx. 65°C until completely melted. When these components are melted, the compound is removed from the heat and a homogenized mixture consisting from a zinc oxyde, talcum powder and paraffin oil is added slowly with constant stirring until completely homogenized. The product obtained by this procedure is cooled down resulting in a mild yellowish ointment with a mild almond scent.
CN103479662A Application of auranofin to preparation of anti-angiogenic medicine The invention relates to application of auranofin to preparation of anti-angiogenic medicines. So far, there is no report on anti-angiogenic activity of auranofin. The invention provides application of auranofin to preparation of anti-angiogenic medicines. A zebra fish angiogenic model is used for verification, and auranofin can substantially inhibit angiogenesis of the zebra fish. Accordingly, auranofin can be used for preparation of anti-angiogenic medicines.
WO2009052454A3 Compositions and methods for ameliorating cns inflammation, psychosis, delirium, ptsd or ptss The invention provides compositions and methods for ameliorating, treating, reversing or preventing pathology or inflammation in the central nervous system (CNS), or the brain, caused or mediated by NFkB, IL-6, IL-6-R, NADPH oxidase (Nox), and/or superoxide and/or hydrogen peroxide production by a NADPH oxidase, including for example ameliorating, treating, reversing or preventing schizophrenia, psychosis, delirium, e.g., post-operative delirium, drug-induced psychosis, psychotic features associated with frailty syndrome (FS), aging, depression, dementias; traumatic war neurosis, post traumatic stress disorder (PTSD) or post-traumatic stress syndrome (PTSS), Amyotrophic Lateral Sclerosis (ALS, or Lou Gehrig's Disease), and/or Multiple Sclerosis (MS). The invention also provides methods for purifying a C60 fullerene, C3 (tris malonic acid C60) or malonic acid derivatives.
EP1326834B1 2-substituted heterocyclic compounds Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds. An example compound has the formula (I).
WO2006134146A1 Orthopaedic skeletal demonstration aids An orthopaedic skeletal demonstration aid for demonstrating surgical orthopaedic techniques comprises a facsimile of part of a vertebral column including five vertebral elements (2) and a sacrum (3) individually moulded from a synthetic material capable of replicating the fine structure of the bone surface so as to correctly reproduce the actual external appearance of the lower part of the human spinal. Adjacent vertebral elements (2) are connected together by connecting portions (9), each of which has a ball (11) at one end and a socket (12) at the other end such that adjacent vertebral elements (2) are interconnected by the ball(11) of the connecting portion (9) of one vertebral element (2) snapping into the socket (12) of the connecting portion (9) of the other vertebral element (2) so as to hold the vertebral elements (2) firmly together whilst enabling articulation of the vertebral elements (2) relative to one another. This has the advantage that each vertebral element (2) is capable of being detached without disturbing the attachment of the other vertebral elements, so as to enable one or more damaged vertebral elements to be replaced so that the aid can be reused. Furthermore the articulation of the vertebral elements relative to one another enables simulation of a plurality of anatomical distortions that occur in the spine, for the purpose of demonstrating a wide range of replacement or repair techniques.
CN101843633B Use of limonium sinense kuntze polysaccharose in preparation of anti-oxidizing medicament The invention relates to the field of natural medicaments and discloses use of limonium sinense kuntze polysaccharose in the preparation of an anti-oxidizing medicament. Pharmacological experiments show that the limonium sinense kuntze polysaccharose has anti-oxidation and anti-tumor functions.
EP2231152A2 Thienopyranones as kinase inhibitors The invention, relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as Pl-3 kinase.
CN102093380B Cyclic icaritin aglycon as well as preparation method and application of cyclic icaritin aglycon The invention discloses cyclic icaritin aglycon the structural formula of which is shown in the specification. The preparation method of the cyclic icaritin aglycon comprises the following steps: (1) smashing dried epimedium or cutting the dried epimedium into segments, adding water and heating for extraction, filtering the extract to obtain concentrated liquor; (2) carrying out macroporous resinchromatography purification on the concentrated liquor, after the macroporous resin fully absorbs the concentrated liquor, eluting with water until the eluent is colourless, removing the eluent, theneluting with 20-50% methyl alcohol or ethanol, collecting the eluent, recovering the alcohol or ethanol, and then drying; and (3) adding a strong acid methyl alcohol or ethanol solution in the obtained dried substance from the step (2), wherein the volume ratio of dried substance to strong acid methyl alcohol or ethanol solution is (2-6): 100, heating and refluxing after fully stirring, recovering the methyl alcohol or ethanol under reduced pressure, extracting the concentration liquor with ethyl acetate, boiling the solvent off so as to obtain the crude cyclic icaritin aglycon. The prepared cyclic icaritin aglycon (the epimedium content is 90%) can be used for resisting oxidation, resisting bacterium, improving cardiovascular, resisting osteoporosis, resisting inflammatory, enhancing immunity and improving estrogen level.
CN1903190A Furosemide injection and its prepn. method A freeze-dried powder injection of frusemide contains frusemide, excipient and heat source removing agent. Its improved preparing process is also disclosed.
US20120052005 Combination therapy to improve drug efficiency Compositions and methods for increasing drug bioavailability and/or preventing multi-drug resistance through inhibition of ABCG2 by xanthine compounds are disclosed.
CA2443950C Inhibition of raf kinase using quinolyl, isoquinolyl or pyridyl ureas This invention relates to a group of quinolyl, isoquinolyl and pyridyl ureas, their use in treating raf mediated diseases, and pharmaceutical compositions which contain these ureas for use in such therapy. These compounds have one of the following formulae: A D B (I) A'-D-B' (II) A"~D~B" (III) wherein D is -NH-C (O)-NH-; A is a substituted pyridyl group; A' is an optionally substituted isoquinolinyl group or a quinolinyl group; A" is a substituted quinolinyl group, B and B' are each, independently, a substituted or unsubstituted bridged cyclic structure of up to 30 carbon atoms; and a cyclic moiety having at least members and B" is a substituted or unsubstituted, up to tricyclic aryl or heteroaryl moiety of up to 30 carbon atoms.
CN102846569A Drug composition containing pirfenidone, and preparation method thereof The present invention belongs to the technical field of medicine, and particularly relates to a solid drug composition containing pirfenidone, and a preparation process thereof. The drug composition contains pirfenidone, a binder and a disintegrating agent, and can be prepared into tablets, granules and capsules.
US20110086894 Biomarkers for the diagnosis of als Methods for determining the onset of ALS in a subject are provided. One method includes analyzing a sample obtained from the subject for the presence or amount of one or more biomarkers indicative of ALS. In a preferred embodiment, the biomarkers are one or more of the following: C-reactive protein (CRP), cystatin c, plasminogen, complement C3, CysGly-transthyretin, and phosphorylated neurofilament heavy chain (pNFH). The sample is typically cerebral spinal fluid (CSF). The levels or concentrations of the biomarkers can be used to determine the onset of ALS, monitor the progression of ALS, or monitor the progression of a treatment for ALS.
US7097998 Aβ42 lowering agents The invention provides a method of preventing, delaying, or reversing the progression of Alzheimer's disease by administering an Aβ42 lowering agent to a mammal under conditions in which levels of Aβ42 are selectively reduced, levels of Aβ38 are increased, and levels of Aβ40 are unchanged. The invention provides methods and materials for developing and identifying Aβ42 lowering agents. In addition, the invention provides methods for identifying agents that increase the risk of developing, or hasten progression of, Alzheimer's disease. The invention also provides compositions of Aβ42 lowering agents and antioxidants, Aβ42 lowering agents and non-selective secretase inhibitors, as well as Aβ42 lowering agents and acetylcholinesterase inhibitors. The invention also provides kits containing Aβ42 lowering agents, antioxidants, non-selective secretase inhibitors, and/or acetylcholinesterase inhibitors as well as instructions related to dose regimens for Aβ42 lowering agents, antioxidants, non-selective secretase inhibitors, and acetylcholinesterase inhibitors.
WO2011103648A1 Method for preparing ointments containing antioxidants from polyphenol-rich plants for use in the treatment of wounds of various origins which involve an increase in oxidation-promoting agents and/or increased formation of oxygen-derived reactive species and/or reduced formation of nitric oxide This invention relates to a method for producing oitnments and/or creams that contain antioxidants from polyphenol-rich plants such as Euterpe oleracea (assai palm), for use in the treatment of wounds, in order to accelerate the cicatrisation process, whenever there is an increase in the formation of oxidation-promoting compounds and a reduced synthesis of nitric oxide.
WO2012091628A3 Substituted hydrogenated thieno-pyrrolo[3,2-c]pyridine, ligands, a pharmaceutical composition and a method for using the above The invention relates to novel substituted tetrahydro-4H-thieno-pyrrolo[3,2-c]pyridines of general formula 1, geometric isomers thereof, mixtures of the geometric isomers thereof, and pharmaceutically acceptable salts thereof, where Th is an annulated thiene ring; W is a single bond (in this case R3 is bonded directly to the nitrogen atom of the pyrrole ring), a methylene, 1,2-ethane, 1,2-ethylene, 1,2-acetylene, 1,3-propane or 1,3-allyl bridge optionally substituted by a hydroxyl group; R1 and R2 are hydrogen, C1-C4alkyl, halogen or -СН2ОН; R3 is hydrogen, optionally substituted phenyl, optionally substituted azaheteroaryl; R4 is C1-C4alkyl, СО2С2Н5 or СО2С(СН3)3; R5, R6, R7, independently of one another, are hydrogen or C1-C4alkyl, or R5 and R6 together form an ethylene bridge and R7 is a hydrogen atom, or R5 and R7 together form an ethylene bridge and R6 is a hydrogen atom; and also to the synthesis of novel chemical substances, novel physiologically active substances, "molecular instruments", a pharmaceutical composition, methods for producing same and a method for treating and preventing the development of various diseases, including diseases of the central nervous system.
US20050100589 Transdermal administration of ace inhibitors Disclosed is a dermal composition comprising enalapril ethyl ester or another prodrug corresponding to a pharmaceutically active form of an ACE inhibitor in an amount corresponding to a therapeutically effective amount of enalaprilat (or other pharmaceutically active form of enalapri) or pharmaceutically active form of the ACE inhibitor in admixture with a pharmaceutically acceptable carrier. In a preferred embodiment, the carrier is a pressure-sensitive adhesive matrix comprising a polymer or polymer blend. The dermal composition is applied in a method of substantially increasing the flux of enalaprilat through the skin of a human or an animal by maintaining the dermal composition in contact with the skin.
CN103073543A Preparation method and application of tropisetron citrate crystal form I The invention discloses a preparation method and an application of a tropisetron citrate crystal form I. The tropisetron citrate crystal form I is obtained through selecting from different crystal solvents and temperatures. The tropisetron citrate crystal form is simple in preparation technology, and has good stability; a sample prepared with the method can effectively reduce residual quantity of introduced solvents, such as methylbenzene, trichloromethane and pyridine in a synthesis process; product purity is better; and industrial production is facilitated.
US20100113374 Methods and related compositions using specific flavonoids and indanes to reduce weight and inhibit lipase, alpha-amylase and alpha-glucosidase activity in mammals The present invention relates generally to methods and related compositions using flavonoids and/or indanes extracted from the stems and leaves of C. quadrangularis to reduce weight and inhibit lipase, α-amylase and α-glucosidase activity in mammals. By example and not by way of limitation, embodiments of the present disclosure, a composition and related methods for reducing body weight and/or inhibiting any combination of lipase, α-amylase and α-glucosidase is provided. The composition contains an effective amount of one or more flavonoids or indanes selected from 3-O-rhamnopyranosylkaempferol, 3-(4-hydroxybenzylidene)-2-(2,5-dihydroxyphenyl)-1-(4-hydroxyphenyl)indane-4,6-diol, quercitrin, rhamnitrin, rhamnocitrin, quercitrin-3-O″-acetate and parthenocissin A.
WO2013109521A1 Pyran-spirocyclic piperidine amides as modulators of ion channels The invention relates to pyran spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
EP1633710A1 Isoindolin-1-one compounds as kinase inhibitors Compounds having the formula, (I) are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds and compositions containing the compounds.
CN1870910B Synbiotic composition for infants There is provided a preparation comprising Bifidobacterium breve and a mixture of non-digestible carbohydrates for non- or partially breast-fed infants as well as the use thereof for the treatment orprevention of immune disorder in non- or partially breast-fed infants. Also provided herein are sequence primers and probe for the detection of Bifidobacterium species as well as diagnostic kit thereof.
CN101314031A Preparation for improving osteotrophy The invention provides a preparation for improving osteotrophy, relating to a calcium supplement product, in particular to a calcium supplement preparation for improving the osteotrophy. The invention is mainly prepared from main materials of calcium carbonate and casein phosphopeptide. The main materials are prepared by weight portion: 10 to 60 portions of calcium carbonate, 1 portion of casein phosphopeptide and 0.1 to 250 portions of auxiliary materials. The formula of the invention is scientific and reasonable and has functions of directly supplementing calcium, promoting calcium absorption, reducing calcium loss, improving the osteotrophy and bone metabolism and increasing bone mineral density.
CN101991689A Pharmaceutical composition for treating skin pruritus The invention discloses a pharmaceutical composition for treating skin pruritus and a preparation method thereof. The pharmaceutical composition is prepared from the raw medical materials, such as radix sophorae flavescentis, golden cypress, fructus cnidii, halloysitum rubrum, borneol, and the like. The preparation method comprises the following steps of: extracting the raw medical materials with ethanol or water, carrying out ultrafinely crushing and other processes to prepare thick paste or thin paste and superfine powder; and adding conventional auxiliary materials according to a conventional process to prepare various external preparations. Accordingly, the pharmaceutical composition of the invention has the functions of reducing fever, removing dampness, killing insects and relieving itching, has accurate curative effect, stable and reliable quality, long service life, portability and convenient use and is particularly suitable for various kinds of skin pruritus.
CN101703723B Drug-breaking medicine and preparation method thereof The invention relates to a drug-breaking medicine and a preparation method thereof, aiming to abstain the physical dependence and psychic dependence of drug addicts on drugs. The drug-breaking medicine is prepared from the following raw materials by weight: 5g of cordyceps sinensis, 6g of open ganoderma spore, 15g of ginseng, 20g of Chinese angelica, 12g of root of hairy asiabell, 9g of liquorice, 25g of gynostemma pentaphyllum, 10g of royal jelly, 9g of datura flower, 18g of processed radix aconite, 1.5g of dried venom of toads, 10g of little multibanded krait, 6g of artificial bezoar, 1.5g of borneol, 15g of Chinese ginger, 10g of rhizoma pinelliae, 25g of spina date seed, 7.5g of ligusticum chuanxiong hort, 30g of white pepper and 12g of rhizoma polygonati. The drug-breaking medicine can be used to fast relieve the abstinence syndrome, have remarkable curative effect on de-addiction treatment of opiates psychiatric drugs and other narcotics psychiatric drugs, and abstain the physical dependence and psychic dependence of drug addicts on drugs.
US20110195945 Compounds, Compositions and Methods for Treating or Preventing Hypoxic or Ischemic Injury Compositions and methods of treating or preventing disease or injury to a human patient or biological material undergoing ischemic or hypoxic conditions.
CN103417831A Medicine curing cough and preparation method thereof The invention discloses a medicine curing cough and a preparation method thereof. The medicine is mainly composed of Arisaema heterophyllum, fructus aurantii, dried orange peel, Chinese magnoliavine, tuber of dwarf lilyturf, anemarrhena and the like according to a certain weight ratio. The medicine has the functions of regulating Qi, strengthening the spleen, clearing away heat, drying dampness, moistening the lungs, descending Qi, preventing phlegm from forming and stopping coughing. The medicine is used for curing the cough, becomes effective rapidly, and is high in cure rate.
US20120141459 Molecular targets for als and related disorders Provided herein are compositions and methods for diagnosis, risk assessment, research, and therapy related to amyotrophic lateral sclerosis (ALS) and ALS-related disorders. In particular, the present invention relates to mutations in the UBQLN2 gene that cause dominantly inherited chromosome X-linked ALS and ALS/dementia.
US7244448 Providing liposome having free active agent and precipitated active agent encapsulated therein; varying amount of active agent that is precipitated in liposome for modulation plasma circulation half-life of active agent This invention relates to liposomal antineoplastic agents (e.g., camptothecin) compositions and methods of using such compositions for treating neoplasia and for inhibiting angiogenesis. The compositions and methods are useful for modulating the plasma circulation half-life of an active agent.
CN1796389A Antibacterial compound A-13, and application in preparing antibacterial drug This invention publishes an antibacterial compound A-13 with a common formula (I), its application in manufacturing antibacterial drugs and its blended composite drugs. This compound, with its pharmacologically permitted ester derivatives, ether derivatives, amino-formyl-N-alkyl derivatives and salts, performs outstanding and broad-spectrum antibacterial activity. It is especially germicidal to leptospiras and some other G- or G+ bacteria and is thus applicable in curing or preventing infection diseases.
WO2013169740A2 Synthetic triterpenoids and methods for modulating stem/progenitor cell gene expression Synthetic triterpenoids and methods of using the same to induce gene expression and differentiation of stem or progenitor cells are provided.
CN101797267A Medical composite for preventing and curing Alzheimer's disease The invention discloses a medical composite for preventing and curing Alzheimer's disease (AD). The composite comprises the following raw materials in parts by weight: 10-40 parts of hyperin, 20-80 parts of icariin and 5-20 parts of Schisandrin B. Experiments of rat place navigation and space exploration prove that the medical composite of the invention can increase the ability of spatial learning and memory of AD rat model, namely reduce the escape latency and scouting distance and obviously increase the percent of scouting time in quadrant of original platform to total time and the percent of scouting distance in quadrant of original platform to total distance in space exploration experiments. Therefore, the extract composite can be used for preventing and curing AD.
WO2013148269A1 Methods and compositions for reducing the proliferation of gram positive bacteria Provided herein are methods for inducing cell death in a gram positive bacterium and methods for reducing the proliferation of a gram positive bacterium that include contacting a gram positive bacterium with a dye (e.g., an azo dye) and a TarO inhibitor. Also provided are methods of treating a subject having a gram positive bacterial infection that include administering to a subject having a gram positive bacterial infection a dye (e.g., an azo dye) and a TarO inhibitor. Also provided are compositions containing a dye (e.g., an azo dye) and a TarO inhibitor, and kits containing at least one of these compositions.
US20110076238 Compounds for the treatment of proliferative processes The invention relates to the use of anticholinergics for preparing a pharmaceutical composition for the prevention and treatment of proliferative processes.
CN102232951A Medicament for treating allergic conjunctivitis and preparation method thereof The invention relates to a medicament for treating allergic conjunctivitis and a preparation method thereof. The medicinal preparation provided by the invention is an eye drop and comprises the following components of: 0.69g of Ketotifen fumarate, 50.00g of mannitol, 2.00ml of a benzalkonium bromide solution at the concentration of 5%, 0.05-0.5g of disodium edentate, a proper amount of a sodium hydroxide solution and injection water which is added to 1000ml.
US7319105 Cytotoxic agents The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for preparing compounds of the invention, and therapeutic methods for treating cancer and other topoisomerase mediated conditions.
US7112580 3-nitrogen-6, 7-dioxygen steroids and uses related thereto A compound of the formula: and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein R groups are as defined by the present specification. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.
US20110027283 Methods for diagnosing and treating cancers This disclosure provides methods and compositions for inhibiting immune responses. The disclosure also provides methods and compositions for inhibiting graft rejection and promoting or prolonging graft survival.
US20060089400 Novel spiro ketone and carboxylic acid derivatives as specific inhibitors for (po3h2) ser/(po3h2)thr-pro-specific peptidyl-prolylcis/trans-isomerases The invention provides new spiro and carboxylic acid derivatives, pharmaceutically compositions comprising them and their use for the preparation of pharmaceutical compositions.
CN101518545B Synthesis and surface decorating method of rare-earth nanometer compound material The invention belongs to the technical field of material chemistry and material physics, and in particular relates to a synthesis and surface modification method of rare-earth nanometer compound materials. The invention prepares the rare-earth nanometer compound materials by the steps of the hydrolysis of butyl titanate, the mixing of element solutions, surface modification, high-temperature calcination, and the like and using a mixing and surface modification technology of rare-earth elements and transitional metal elements. Under the irradiating illumination of near infrared lights or visible lights, and the rare-earth elements generate upconversion luminescence to excite titanium oxide to achieve anti-bacterium and anti-tumor functions. The invention has the characteristics of simple material synthesis method, multiple preparation technologies, easy-controlled combination, low cost, good modified effect on titanium oxide, and the like, does not pollute or harm the human and the environment, can directly kill bacteria and tumors and decompose the endotoxin generated by the bacteria and the tumors, and does not need secondary processing.
CN1842527A Paroxetine cholate or cholic acid derivative salts, and composition comprising paroxetine and cholic acid or chlolic acid derivatives Disclosed herein is a paroxetine cholate or cholic acid derivative salt and a composition comprising paroxetine and cholic acid or a derivative thereof. Further disclosed is a pharmaceutical composition comprising the paroxetine salt or the composition. The pharmaceutical composition can be formulated into an oral preparation for swallowing without water as an orally disintegrating tablet for paroxetine.
WO2006076240A2 Compositions, products and methods for controlling weight in a mammal Compositions for controlling mammalian weight, said compositions comprising one or more lipolytic agents for stimulating mammalian lipolysis and/or thermogenic agents for modulating mammalian thermogenesis. Products, consumer and otherwise, comprising said compositions and methods of using both the present compositions and products to control mammalian weight.
WO2008124838A1 Compounds that inhibit human dna ligases and methods of treating cancer Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.
US20100286031 Antibiotic Formulations, Unit Doses, Kits and Methods An aqueous or powder composition includes anti-gram-negative antibiotic or salt thereof being present at an amount ranging from about 100 mg/ml to about 200 mg/ml. Another aqueous or powder composition includes anti-gram-positive antibiotic or salt thereof being present at a concentration ranging from about 0.6 to about 0.9 of the water solubility limit, at 25° C. and 1.0 atmosphere, of the anti-gram-positive antibiotic or salt thereof. Other embodiments include unit doses, kits, and methods.
CN1559433A Polyhexose type nanometer antimicrobial matter, prepn. method and use thereof A polyose-type nano-class antibacterial material used for medicines or as the additive of feed is prepared from chitosan and bactericiding metal ions.
EP1255553B1 Use of trilostane or keto-trilostane in combination with an antioestrogen in the treatment of a hormone-dependent condition. Use of a compound of formula (I) or a 3-enol C1 to 4 alkanoate ester thereof in the manufacture of a medicament for the treatment of a hormone dependant condition by modulation of the oestrogen receptor β (ERβ) wherein R1, R2, R5 and R6 are the same or different and each is hydrogen or C1 to 4 alkyl; R3 is hydrogen, C1 to 4 alkyl, C1 to 4 alkenyl or C1 to 4 alkynyl; R4 is hydroxy, C1 to 4 alkanoyloxy, a group of formula (II) or (III) wherein R7 is (CH2)n, where n is an integer of from 0 to 4, R8 is hydrogen, C1 to 4 alkyl, hydroxy or NH2 and R9 and R10 are the same or different and each is hydrogen or C1 to 4 alkyl; or R3 and R4 together are oxo, ethylenedioxy or propylenedioxy.
WO2006132204A1 Transcription factor decoy Disclosed are: a double-stranded oligonucleotide which is useful as a decoy oligonucleotide having a high ability to bind to a transcription factor and a reduced cytotoxicity; and use of the double-stranded oligonucleotide for medical purposes. A double-stranded oligonucleotide composed of a hybrid of a sense oligonucleotide having a nucleotide sequence depicted by the formula A with an anti-sense oligonucleotide which is complementary to the sense oligonucleotide: 5'-N(m)-G-(consensus sequence)-C-N(n)-3' (A) wherein N(m) represents a sequence which is added to the 5'-terminus and is composed of m units of N's and N(n) represents a sequence which is added to the 3'-terminus and is composed of n units of N's, wherein all of N's independently represent a nucleotide A, G, T, C or U; m and n independently represent an integer of 0 to 20; and the term 'consensus sequence' means a consensus sequence to which a transcription factor is to be bound.
EP1719543A1 Use of histone deacetylase inhibitors for the treatment of gastrointestinal distress Use of a pharmaceutical composition for the manufacture of a medicament for treating and/or preventing acute and chronic gastrointestinal distress including nausea, vomiting, lactose intolerance, obstructive symptoms, diarrhea, mucositis, bleeding, weight loss, and malnutrition in a subject who is immunocompromised or receives a planned course of chemotherapy and/or radiotherapy. The pharmaceutical composition comprises a histone deacetylase inhibitor optionally in conjunction with a second agent. It is further provided use of a histone deacetylase inhibitor for the manufacture of a medicament for treating and/or preventing cachexia, cancer-related fatigue, or chronic fatigue syndrome.
CN101879175A Dashing agent of ivermectin and levamisole and preparation method thereof The invention discloses a dashing agent of ivermectin and levamisole for preventing and controlling in vivo and in vitro parasites. According to the formula, the dashing agent comprises the following components in percentage by w/v: 0.5 to 1 percent of ivermectin, 5 to 10 percent of levamisole, 20 to 50 percent of octyl-decyl glycerate, 1 to 3 percent of oily laurocapram and the balance of medicinal soybean oil, wherein in the formula, v is a volume unit ml, and w is a weight unit g; and the ivermectin is anti-parasitic agent, the levamisole is vermifuge, both the ivermectin and the levamisole have immunological enhancement effects, the octyl-decyl glycerate is medicament dissolving agent, the oily laurocapram is transdermal absorption promoter and the medicinal soybean oil is oily diluent. The dashing agent of the ivermectin and the levamisole has wide application range, can be used for big animals, small animals and economic animals, has a simple administration method, is directly dashed or coated on a sick part, is particularly suitable for wild grazed cattle and sheep, is a medicament which cannot be flushed away by rainwater and snow water, and has unmatched advantages compared with water-based liniment.
EP2379100A1 Method for treating hyperglycemia with glp-1 A method for treating hyperglycemia and/or diabetes in a subject is provided. In particular, the method is directed for the treatment of patients with type 2 diabetes mellitus who have a fasting blood glucose concentration greater than about 8 mM, wherein the patient is administered a formulation comprising a GLP-1 molecule and a diketopiperazine by pulmonary inhalation with a dry powder inhalation system.
WO2011092720A3 Pharmaceutical composition of prasugrel and its pharmaceutically acceptable salts and process for their preparation A pharmaceutical composition of prasugrel or its pharmaceutically acceptable salts, especially hydrochloride salts as well as process for their preparation are provided. The pharmaceutical composition comprises: a) prasugrel hydrochloride, b) a water insoluble dry binder, c) at least one diluent, d )at least one disintegrant and e) at least one lubricant. The pharmaceutical composition is optionally coated with a film. An improved process for preparing of prasugrel and its pharmaceutically acceptable salts, a process for purifying 5,6,7,7a-tetrahydro-4H-thieno[3,2-c]pyridine-2 -one hydrochloride compound, a process for preparing crystalline form-B2 of prasugrel hydrochloride and a process for preparing a-cyclopropylcarbonyl-2-fluorobenzyl bromide compound are provided.
CN1994387A Pharmaceutical composition for treating acne and beautifying face The invention discloses a pharmaceutical composition having beauty treatment effect for treating acne, which comprises rhubarb horsetails, root of red rooted saliva, astragalus root, gingko, citron fruit, red halloysite, licorice root, borneo camphor and momordica seed. The prepared composition has the advantages of low cost, short course of treatment, higher curing rate, and low recurrence rate.
WO2011129424A1 Pharmaceutical agent for prevention and/or treatment of htlv-1-associated myelopathy Disclosed is a therapeutic agent for HTLV-1-associated diseases such as HTLV-1-associated myelopathy and uveitides. Specifically disclosed is a pharmaceutical agent comprising, as an active ingredient, an RAR agonist represented by formula (I) [wherein R1 to R5 independently represent a hydrogen atom, an alkyl group, or an alkyl-substituted silyl group; X represents -CO-NH-, -NH-CO- or -CO-CH=CH-; and A represents a carboxylate-substituted aromatic group or a tropolonyl group].
EP1458725B1 A novel sordarin derivative isolated from culture fermentations and functions as an antifungal agent A novel sordarin derivative was isolated from fungal cultures. The compound is useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops. Two novel cultures of fungi, ATCC No. PTA-3862 and ATCC No. PTA-3861 can be used to ferment and produce the present compound.
US8791079 Methods for treating heart failure by inhibiting the mitochondrial sodium-calcium exchanger (mNCE) Methods and compounds for preventing or reducing the toxic side effects of cardiac glycosides by inhibiting the mitochondrial sodium-calcium exchanger (mNCE) are provided. Methods and compositions for preventing or reducing the occurrence of conditions associated with heart failure, including, but not limited to, sudden cardiac death and contractile decompensation, by inhibiting the mNCE also are provided.
CN102961322A Drug-loaded mixed micelle The invention discloses a drug-loaded mixed micelle comprising taxane medicaments, amphiphilic chitosan derivatives and polyethylene glycol polyester block copolymer. The invention further discloses a preparation method of the drug-loaded mixed micelle. The product does not contain polyoxyethylene castor oil and ethanol, reduces adverse drug reactions, increases security of drug clinic application; by adding the amphiphilic chitosan derivatives and the polyethylene glycol polyester block copolymer, the stability of the preparation is enhanced and drug loading and drug efficacy are increased; and the preparation process is simple and controllable, and the production can be expanded easily.
EP2351737A1 3-Amino-1-arylpropyl indoles and aza-substituted indoles The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds
CA2225807C Use of lamellarin-class alkaloids in methods of treatment The lamellarin compounds disclosed herein have been found to be inhibitors of MDR, i.e., acquired multidrug resistance, which has become a major problem in the treatment of various cancers. The lamellarin compounds disclosed herein have also been found to be cytotoxic to MDR cells. MDR is believed to be associated with certain alterations in tumor cells, including an over-expression of a certain high molecular weight membrane glycoprotein and a decrease in the ability of the tumor cell to accumulate and retain chemotherapeutic agents. The present invention is thus directed to methods of treating MDR-type tumors with an effective anti-MDR amount (either inhibitory or cytotoxic) of one or more lamellarin compounds, which compounds have been found to be effective antitumoral agents against MDR cells.
CN1965974A Medicament for treating psoriasis, preparation process and using method thereof Disclosed is a medicament for treating psoriasis wherein the oral medicament comprises the following raw materials: frankincense, myrrh, linaloe, banksia rose, dragon's blood resin, black catechu, silver flower, wild chrysanthemum flower, and kansui root. The medicine for external application includes formula I and formula II, wherein formula I comprises ledebouriella root, flavescent sophora root, cantharis, licorice root, areca-nut, carpesium fruit, pricklyash peel, aniseed, scrophularia root, Chinese angelica root, Cinnamomum cassia, dahurian angelica root, rhubarb horsetails, radix paeoniae rubrathe, dried rehmannia root, Schizonepeta tenuifolia, momordica seed, cnidium fruit, buthus martensi karsch, cicada shell, hibiscus bark, croton, and atractylodes rhizome, the formula II comprises orpiment, Cinnamomum camphora, dried alum, radix euphorbiae ebracteolatae, Chinese honey locust and apricot seeds.
CN102813753A Composition containing Cistanche deserticola or Herba Cynomorii and combination of chrysanthemum, taurine, lycopene, xanthophyll and beta-carotene The invention relates to a nutritional food and a medicine, and especially relates to a composition which can alleviate the eye fatigue, improve the eyesight, reduce the blood fat and nourish the liver and the kidney, has no toxic side effects and is suitable for long-term taking. The composition comprises the following components, by weight, 100-900 parts of Cistanche deserticola or Cistanche deserticola, and one or several of 200-1000 parts of chrysanthemum, 200-2000 parts of taurine, 5-30 parts of lycopene or 5-30 parts of astaxanthin or 100-900 parts of grape pip, 2.5-15 parts of beta-carotene or a Dunaliella salina extract, and 6-30 parts of xanthophyll.
CN102872089A Application of Houttuynoid E in medicines for treating skin cancer The invention discloses an application of Houttuynoid E in preparing medicines for treating skin cancer, and belongs to the technical field of new applications of medicines. In vitro MTT (Methyl Thiazolyl Tetrazolium) antineoplastic activity evaluation finds that Houttuynoid E has remarkable inhibition effect on the growth of human skin cancer cell lines A431, HME1, A375 and SK23, so that Houttuynoid E can be used to prepare medicines for inhibiting skin cancer and has good development application prospect. The application of Houttuynoid E in medicines for treating skin cancer is disclosed for the first time, and has extremely high inhibitory activity to skin cancer cells as the skeleton type belongs to a completely novel skeleton type.
CN101744787A Controlled release composite containing vinpocetine The invention relates to a controlled release composite containing vinpocetine, which is a vinpocetine controlled release tablet. If taken once or twice a day, the vinpocetine controlled release tablet can release drug at a constant speed and relieve in vivo blood concentration fluctuation. The vinpocetine controlled release tablet is a single-chamber osmotic pump which has two parts in structureand consists of a drug core containing the vinpocetine and a semipermeable film which has small holes and can be only permeated by water and other micromolecules.
US20110053994 Potent immunosuppressive agents, derivatives and uses Provided herein include compositions, all related stereoisomers as well as pharmaceutically acceptable salts provided as simplified analogs of pateamine A, in which the analogs generally are devoid of the C3-amino and C5-methyl groups, also referred to as desmethyl, desamino-pateamine A. Suitable analogs provide anticancer and antiproliferative effects in vivo and in vitro by a novel drugs mechanism of action described herein for pateamine A, including inhibition of eIF4A-dependent translation initiation. As with pateamine A, as described herein, suitable analogs cause cell cycle arrest or induce apoptosis in transformed cells. However, toxicity of such compounds to slow growing normal cells is low. In addition, such analogs, like pateamine A, target translation initiation factors and are useful as anticancer and antiproliferative agents in subjects in need thereof. Moreover, the analogs, like pateamine A, are valuable molecular probes for evalutaion of eukaryotic translation initiation and as lead compounds for development of improved anticancer agents.
US20120270953 Methods and compositions for the treatment of infection or infectious colonization of the eyelid, ocular surface, skin or ear The instant invention provides methods and compositions for the treatment of infection or infectious colonization of the eyelid and/or ocular surface for the treatment and prevention of ocular disorders and eyelid disorders.
CN103145740A Sulfoxide alkaloid compound as well as preparation method and application for same The invention discloses a sulfoxide alkaloid compound as well as a preparation method and an application for the same, and belongs to the field of microbial technology. The sulfoxide alkaloid compound is obtained by inoculating marine streptomyces into a tryptone soy broth liquid culture medium, culturing for 48-72 hours at a temperature of 28-30 DEG C and with a speed of 180-200 rpm, inoculating the marine streptomyces into a fermentation culture medium according to 10% of inoculum size, culturing for 432-456 hours at a temperature of 28-30 DEG C and with a speed of 180-200 rpm, and separating and purifying the fermentation solution. The compound has a remarkable inhibition effect on various bacteria, in particular, on staphylococcus aureus, and a certain anti-tumour activity for human breast cancer cells MCF-7, human liver cancer cells SMMC-7721, human acute myelomatosis cells U937 and small cell lung cancer cells NCI-H1688 simultaneously. Therefore, the compound has a good prospect for developing new anti-cancer medicines and new antibacterial medicines.
CN102100671A Method for preparing esomeprazole enteric capsules The invention discloses a method for preparing esomeprazole enteric capsules. The method comprises the steps of the preparation of active pellets of esomeprazole, coating of an isolation layer and coating of an enteric layer, wherein sodium stearyl fumarate is used as a strong hydrophilic lubricant. The esomeprazole enteric capsules prepared by the method are quite high in stability.
CA2628794C Treatment of length dependent neuropathy Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with .alpha.-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.
US20050084548 Antiobestic and/or antidiabetic agent containing cyanidin 3-glucoside as active ingredient The invention provides an antiobestic and/or antidiabetic agent containing cyanidin 3-glucoside as an active ingredient. Thereby the increase of adipose cells can be suppressed and the blood glucose level can be reduced safely and effectively.
WO2011130834A8 Non-intravenous dosage form comprising solid formulation of liquid biologically active agent and uses thereof The disclosure relates to a non-intravenous dosage for administration of a liquid biologically active agent. The dosage form contains a solid formulation of the liquid biologically active agent, e.g. propofol, in intimate association with at least one stabilizing agent, e.g. an amphiphilic polymer or surfactant. A liquid biologically active agent is converted to a solid product, e.g. a powder, that can be easily incorporated into a number of different non-intravenous dosage forms. Upon hydration, a nanodispersion or micelle loaded with the active agent is formed. The dosage form can provide a non-intravenous route of administration for active agents that are typically only administered intravenously. Methods, uses, kits and commercial packages related to the non-intravenous dosage form are also disclosed.
CN103301270A Medicine for preventing and treating coronary heart disease and preparation method thereof The invention discloses a medicine for preventing and treating coronary heart diseases and a preparation method of the medicine. The medicine comprises the following components: 1 part of rheum officinale, 1 part of cistanche, 7 parts of the root of kudzu vine, 3 parts of caulis spatholobi, 3 parts of earthworm, 1 part of ginseng, 1 part of pseudo-ginseng, 1 part of zaocys dhumnade, 1 part of concha haliotidis, 1 part of ochre, 1 part of caltrop, 7 parts of uncaria, 7 parts of astragalus membranaceus, 2 parts of scorpion, 1 part of semen cassiae, 7 parts of prunella vulgaris and 1 part of calamus. According to the medicine, all of the raw materials are free of toxic and side effects, the rheum officinale, the prunella vulgaris and the glycerinum are used as the main raw materials, and the other materials are used as the auxiliary materials. The medicine has the effects of invigorating the circulation of blood, dispersing blood stasis, promoting the circulation of qi, eliminating phlegm and relieving pain, and is used for improving corona-arterial blood circulation and treating diseases of hypertension, high cholesterol, coronary heart diseases, angina and the like.
CN102228452A Honokiol or magnolol or honokiol-magnolol mixed solid lipid nanosphere preparation and preparation method thereof The invention relates to a honokiol or magnolol or honokiol-magnolol mixed solid lipid nanosphere preparation and a preparation method thereof. According to the invention, the production problem of the honokiol or magnolol or honokiol-magnolol mixed solid lipid nanosphere preparation can be effectively solved. The raw materials of the honokiol or magnolol or honokiol-magnolol mixed solid lipid nanosphere preparation comprise 0.001-40 wt% of honokiol or magnolol or the honokiol-magnolol mixture, 0.05-99.9 wt% of the solid lipid material, 0.001-85 wt% of a surfactant, and the balance being disperse medium, wherein the sum of the weight of honokiol or magnolol or the honokiol-magnolol mixture, the solid lipid material and the surfactant accounts for 0.01-60% of the total weight of the lipid nanosphere preparation. The preparation method provided by the invention comprises the following steps of: preparing a dispersed phase, preparing a continuous phase, mixing the dispersed phase and the continuous phase, dispersing the mixture to a nanometer preparation, filtering and sterilizing. The honokiol or magnolol or honokiol-magnolol mixed solid lipid nanosphere preparation has advantages of scientific composition, simple preparation and good stability, can be prepared in the forms of an injection and an ophthalmic preparation, or processed in the forms of a solid preparation, a semisolid preparation and a gas preparation.
US7605183 Using 4,4-dimethyl-6-methylene-2-cyclohexen -1-one A method for inhibiting or blocking molecular generating and/or inducing functions of molecules using an inhibitory or blocking agent of the formula: wherein R1-6 are as defined herein.
CN1654041B Application of eagle-tea extract total flavone in preparation of medicine for regulating blood fat The present invention is the application of total flavone of water Litsea coreana extractive in preparing medicine for regulating blood fat. The total flavone of water Litsea coreana extractive has obvious effect of lowering serum triglyceride. The present invention has the advantages of convenient oral taking, less toxic side effect and determined curative effect, is suitable for various kinds ofhyperlipemia, and may be developed into medicine and health article.
EP2344146A1 Use of anti-connexin agents for modulating the therapeutic effect of psychotropic drugs The invention first relates to a product containing at least one connexin-blocking agent and a psychotropic drug as combination products for use simultaneously, separately, or spread over time in patients suffering from psychiatric and/or neurodegenerative disorders. The connexin-blocking agent is advantageously selected from the group comprising meclofenamic acid, 18-β-glycyrrhetinic acid, carbenoxolone, mefloquine, and 2-APB, and preferably consists of meclofenamic acid.
EP2373631A2 Antibacterial compounds Disclosed are compounds of formula (I), which are of use in the treatment of bacterial diseases and infections, to compositions containing those compounds and to methods of treating bacterial diseases and infections using the compounds. In particular, the compounds are useful for the treatment of infection with, and diseases caused by, Clostridium difficile.
US20140100238 Method of diagnosing and treating epstein barr virus-based myalgic encephalomyelitis chronic fatigue syndrome patients A method of diagnosing a subset of Epstein Barr Virus, Myalgic Encephalomyelitis Chronic Fatigue Syndrome (ME/CFS) patients through a multi-prong clinical/serological analysis is provided wherein Epstein Barr Virus Abortive Lytic Replication (EBV) is determined as the specific causal agent through the use of serum antibodies to EBV encoded dUTPase and serum antibodies to EBV DNA Polymerase as molecular markers. A method of treating patients diagnosed with Epstein Barr Virus Abortive Lytic Replication (EBV), Myalgic Encephalomyelitis Chronic Fatigue Syndrome (ME/CFS) with specific antiviral nucleosides is also provided, to alleviate the condition.
WO2011086126A1 Compounds for the treatment of autism The present invention relates to a compound which inhibits the importation of chloride into neurons and a compound which improve the outflow of chloride from neurons for the use in treatment of autism. The invention also relates to a pharmaceutical composition for use in the treatment of autism comprising a compound according to the invention and a pharmaceutically acceptable carrier.
WO2009004584A1 3-aza-bicyclo[3.3.0]octane compounds The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.
CN101926978A Medicine composition for promoting bone and bony articulation health The invention provides a medicine composition for promoting bone and bony articulation health. The medicine composition is a preparation made by main raw materials of oyster and hydrolysis collagen as well as one or more than one of epimedium herb, rhizome drynariae, teasel root, wolfberry, fructooligosaccharide and vitamin. The composition has synergism, animal test shows that the composition has obvious effect on a model of osteoporosis rat induced by ovary removal and has obvious inhibiting effect on rat foot claw swelling induced by carrageenan and rat adjuvant type arthritis. The preparation treats both principal and secondary aspect of disease and is used for preventing and treating osteoporosis, osteoproliferation and ostarthritis.
EP1968566A1 Compositions of cis-9, trans-11 conjugated linoleic acid and vaccenic acid and uses thereof The invention relates to use of the cis-9, trans-11 isomer of conjugated linoleic acid or a salt or ester thereof (cis-9, trans-11 CLA) and vaccenic acid or a salt or ester thereof (VA) to treat or prevent conditions associated with one or more of leukocyte infiltration, eosinophilia, airway remodelling, bronchoconstriction, mucus hypersecretion, and lung and skin inflammation. The present invention also relates to a composition comprising cis-9, trans-11 CLA and VA and use of the composition to treat or prevent conditions associated with one or more of leukocyte infiltration, eosinophilia, airway remodelling, bronchoconstriction, mucus hypersecretion, and lung and skin inflammation. In particular, the medicinal uses, compositions and methods of the invention may be used to treat or prevent conditions such as asthma and dermatitis, and related disorders.
US20130039968 Materials and processes for producing antitoxic fabrics The invention provides a novel method of generating fabrics with outstanding antitoxic properties. The antitoxic properties are imparted to the fabric by introducing an active agent such as an antimicrobial or antiviral agent to the fabric. The active agent may be introduced into the fabric at multiple stages of the manufacturing process. For nonwoven fabrics, the active agent can be introduced during web formation and/or during post-processing steps. The fabrics produced in accordance with the present invention have widespread utility. For instance, they can be used as wound dressings, gowns, drapes, air filters, protective clothing and wipes.
WO2005105062A3 2-methylthiazolidine-2,4-dicarboxylic acid-containing combination preparations The invention relates to a combination preparation from 2-methylthiazolidine-2,4-dicarboxylic acid and/or the physiologically acceptable salts of said compound and at least one anti-angiogenic and/or cytotoxic and/or cytostatic compound. The invention also relates to the use of said combination preparations in the treatment of cancer.
CN101164619A Pyritinol injection with special purpose solvent The present invention belongs to the field of medicine technology, and discloses an injection preparation of pyritinol or its pharmaceutically-acceptable salt with matched special solvent. The injection preparation of pyritinol or its pharmaceutically-acceptable salt is a sterile powder or sterile strong solution which can be prepared or diluted into solution or suspension before clinical application, said sterile solution, emulsion or suspension can be injected into human body interior. The main component of said special solvent is an alkaline compound of alkali metal, it is one kind selected from sodium hydroxide, potassium of hydroxide, oxide of sodium or potassium, sodium carbonate, sodium hydrogen carbonate, potassium carbonate and potassium hydrogen carbonate or several kinds of them. The application of said matched special-purpose solvent can greatly reduce irritation of injection preparation of pyritinol or its pharmaceutically-acceptable salt to the blood vessel, can obviously raise tolerance of patient and safety of clinical application.
US20090088457 Primary Amines as Renin Inhibitors The invention relates to novel primary amine derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
US20070134255 Hmpv treatment with ribavirin and anti-hmpv antibody The invention relates to antimicrobial agents and antibodies and compositions comprising such agents and antibodies to treat and/or prevent respiratory and related diseases, in particular those caused by human metapneumovirus. Provided is a method for treating or preventing respiratory tract infections in a subject infected with a mammalian MPV, said method comprising administering a nucleoside analog, preferably Ribavirin or a derivative thereof, and an antimicrobial neutralising antibody, preferably an anti-hMPV antibody to said subject, and use of said nucleoside analog and antimicrobial neutralising antibody for the manufacture of a medicament for treating or preventing respiratory tract infections in a subject infected with a mammalian MPV.
US20050256194 Denaturants for sympathomimetic amine salts The instant invention makes impractical the use of sympathomimetic amine compositions in illicit drug production. More specifically, the preparation of methamphetamine from the disclosed pseudoephedrine hydrochloride formulations is inhibited. The present invention defines pharmaceutical compositions comprising a sympathomimetic amine salt and at least one combination inhibitor, the combination inhibitor which acts both to interfere with the isolation of the sympathomimetic amine from the composition and to interfere with the conversion of the sympathomimetic amine to another pharmacologically active compound. The contemplated compositions may also include reaction and separation inhibitors in any mixture to assure maximum protection against the use of the sympathomimetic amine-containing compositions for illegal drug manufacture. The presence of the combination, reaction and separation inhibitors does not significantly alter the release of the sympathomimetic amine from the composition.
WO2009107322A1 Pharmaceutical composition for treatment of cancer Disclosed is a pharmaceutical composition which is effective as a therapeutic agent for cancer which requires an iron ion for its expansion, particularly liver cancer. Specifically disclosed is a pharmaceutical composition which comprises, as an active ingredient, deferoxamine which is one of the iron chelating agents that have been used as therapeutic agents for hemochromatosis. The pharmaceutical composition is effective as a therapeutic agent for liver cancer.
US20050239754 S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine salicylate monohydrate crystalline salt A crystalline salicylate monohydrate salt of S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine is disclosed. A method to make crystalline S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine is further disclosed. In addition, methods of use for crystalline S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine are disclosed
US7214674 Heterocyclymethylpiperidines and -piperazines possessing affinity at 5ht-1 type receptors Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH2 or oxygen and is a single bond; or X is nitrogen, Y is CH2 and is a single bond; R 1 is halogen, cyano, or C1-6 alkoxy; a is 0,1, 2 or 3 ; b is 0 or 1 ; R 2 is hydrogen, C1-6 alkyl, C1-6 alkanoyl, fluoroC1-6 alkanoyl, C1-6 alkylsulfonyl, fluoroC1-6 alkylsulfonyl, carbamoyl, C1-6 alkylcarbamoyl or arylC1-6 alkyl; and R 3 , together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.
CN102552816A Plaster for treating pain and preparation method thereof The invention relates to a plaster for treating pain and a preparation method thereof. The plaster for treating pain comprises the following raw medicinal materials: 5-15g of Herba Daturae seeds, 25-35g of Radix Angelicae, 40-50g of Radix Saposhnikoviae, 40-50g of Carthami Flos, 15-25g of Rhizoma Kaempferiae, 25-35g of Olibanum, 40-50g of Rhizoma Ligustici Chuanxiong, 15-25g of Rhizoma Gastrodiae, 20-40g of Curcuma Rhizome, 20-40g of Cortex Cinnamomi, 10-20g of Radix Inulae, yellow lead with the weight equal to the weight of all above medicinal materials, and cotton oil with the weight twice of the weight of yellow lead. The plaster of the invention is stuck in affected parts or acupuncture points, has the effects of promoting blood circulation and removing stasis, relieving swelling and pain, relaxing tendons and collaterals, and expelling wind and cold, and is used for treatment of soft tissue injuries, tendonitis, tenosynovitis, rheumatism, rheumatoid disease, arthritis, scapulohumeral periarthritis, cervical spondylosis, lumbar disease, lumbar disc herniation, hyperosteogeny, hemiplegia and so on.
WO2008140335A3 Methods of immune or hematological enhancement, inhibiting tumour formation or growth, and treating or preventing cancer, cancer symptoms, or the symptoms of cancer treatments The present invention relates to administration of milk fat or a milk fat analogue, optionally with at least one additional therapeutic factor, preferably lactoferrin or metal ion lactoferrin, preferably iron lactoferrin, preferably bovine lactoferrin, preferably iron bovine lactoferrin, or a metal ion functional variant or functional fragment thereof, to inhibit tumour formation or growth, maintain or improve one or more of the white blood cell count, the red blood cell count, or the myeloid cell count, reduce cachexia, mucositis, and anemia, stimulate the immune system and treat or prevent cancer and the symptoms of cancer and side-effects of cancer therapies. The methods and medicinal uses of the invention may be carried out by employing dietary (as foods or food supplements), nutraceutical or pharmaceutical compositions. Compositions useful in the methods of the invention are also provided.
US7365066 Pyrazolopyridine derivatives as pharmaceutical agents Novel pyrazolopyridine derivative compounds are disclosed and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors useful in the treatment of cancer and other disease states influenced by TGF beta.
CN102766262A Preparation method for difunctional nanoparticle carrier and preparation method for difunctional nanoparticle preparation The invention discloses a preparation method for a difunctional nanoparticle carrier and a preparation method for a difunctional nanoparticle preparation. The preparation method for the difunctional nanoparticle carrier comprises the following steps of: synthesizing ester with formyl by using poly(lactic-co-glycolic acid)-COOH (PLGA-COOH) and p-hydroxybenzaldehyde as raw materials in the presence of 4-dimethylaminopyridine and a condensing agent; synthesizing a PLGA derivative with an acid-sensitive connecting segment hydrazone bond by using the ester with the formyl and carboxyl phenylhydrazine in the presence of p-toluenesulfonic acid; conjugating NH2-polyethylene glycol (PEG)-NH2 and the PLGA derivative with the acid-sensitive connecting segment hydrazone bond in the presence of N-hydroxysuccinimide (NHS) and the condensing agent; and adding folate, the NHS and the condensing agent, and conjugating again to obtain the difunctional nanoparticle carrier PLGA-PEG-folate. The prepared difunctional nanoparticle carrier shows a good pharmacokinetic behavior in vitro, and has high medicine-loading rate, encapsulation rate and stability.
WO2012139507A1 Application of bisphenol fluorene and derivative thereof in preparing medicament for prophylaxis and treatment of cancer An application of bisphenol fluorene and a derivative thereof in preparing a medicament for prophylaxis and treatment of cancer. The compound being an inverse agonist for an estrogen receptor and an estrogen receptor-related receptor, capable of inhibiting effectively estrogen-positive cancer cell growth, thus effectively treating cancers having estrogen-stimulated growth effect such as breast cancer, ovarian cancer, endometrial cancer, cervical cancer, prostate cancer, colon cancer, and lung cancer.
CN103519183A Health food for auxiliary protection against chemical liver injury The invention discloses a health food for auxiliary protection against chemical liver injury. The health food is mainly made of schisandrin B, taurine and vitamin C.
WO2013180462A1 A composition comprising the extract of pine tree leaf or the compounds isolated therefrom for the prevention and treatment of cancer disease by inhibiting hpv virus and the uses thereby The present invention is related to the inventive compositions comprising the extract of pine leaf extract or the compound isolated therefrom. It showed potent inhibitory effect on human papillomavirus (HPV) as well as anti-cancer effect on various cancer diseases through various in vitro test and in vivo tests, and therefore, it can be used as the effective and safe therapeutics or health food for treating and preventing cancer disease.
CN103159711A Once preparation method of composite of 17-hydrogen-9-dehydro-andrographolidume-3, 19-sodium (or potassium) disulfate and 17-hydrogen-9-dehydro-andrographolidume-19-sodium (or potassium) disulfate, and purposes of prepared medicine The invention relates to a composite of 17-hydrogen-9-dehydro-andrographolidume-3, 19-sodium (or potassium) disulfate and 17-hydrogen-9-dehydro-andrographolidume-19-sodium (or potassium) disulfate, and discloses components of the composite and a once preparation method of the components. The composite can be used for preparing medicine having antipyretic, anti-inflammatory and antiviral purposes. The composite is made into dosage forms which can be accepted pharmaceutically.
US20100130594 Cns gene delivery using peripheral administration of aav vectors The present invention relates to compositions and methods for the delivery of therapeutic proteins to the CNS using recombinant AAV vectors. More specifically, the invention relates to compositions and methods for delivering proteins into the cerebrospinal fluid of mammalian subjects through peripheral administration of AAV vectors. The invention may be used to treat various disorders of the central nervous system, including degenerative diseases and motor neuron diseases.
CN101879187A Lamina burn and scald plaster for expelling pus and promoting granulation and preparation method thereof The invention discloses a lamina burn and scald plaster for expelling pus and promoting granulation and a preparation method thereof. The lamina burn and scald plaster is prepared by combining calomel, phlobaphene, mercuric sulphide wool grease, borneol and Vaseline; and the preparation method comprises the following steps of: uniformly mixing the phlobaphene, the mercuric sulphide and the wool grease solid according to a proper part and pulverizing the mixture into fine powder; heating and uniformly stirring the mixture in the fully dissolved vaseline; melting the mixture while heating; and cooling and sub-packaging the mixture to obtain the product.
EP2640355A1 Stable oral pharmaceutical compositions of montelukast A stable liquid oral pharmaceutical composition comprising montelukast, a vehicle comprising mineral oil, desiccant and optionally pharmaceutically acceptable additives is provided. The invention also relates to kit for dispensing of oral pharmaceutical compositions of Montelukast. The kit comprises montelukast, a vehicle comprising mineral oil, desiccant and optionally pharmaceutically acceptable additives. The kit comprises a first container comprising pharmaceutical composition of montelukast and optionally desiccant, a second container comprising a vehicle comprising mineral oil, optionally desiccant and pharmaceutically acceptable additives, and instructions for use. montelukast and mineral oil occupy pre-measured volume into the respective unit of the kit.
US20050164976 Combination of a cdk inhibitor and 5-fu for the tratment of cancer A first aspect of the invention relates to a combination comprising a CDK inhibitor and 5-FU, or a prodrug thereof. A second aspect of the invention relates to a pharmaceutical product comprising a CDK inhibitor and 5-FU, or a prodrug thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a CDK inhibitor and 5-FU, or a prodrug thereof, to a subject.
WO2007117175A1 Pharmaceutical composition of enterosorbent and prebiotics, dosage forms, and the method for prevention and treatment of gastrointestinal disorders The pharmaceutical composition is a combination of hydrolytic lignin with moisture of 55% to 65% consisting of the particles measuring 0.15 mm to 0.55 mm, a 45% to 55% aqueous lactulose solution, and a 50% to 55% aqueous oligosaccharide solution at the following ingredient ratio (weight percent): an aqueous lactulose solution: 10÷60; oligosaccharides: 10÷50; hydrolytic lignin: quantity sufficient. Hydrolytic lignin, lactulose and fructose oligosaccharides are sequentially added and mixed using a rotor blender. The composition is administered orally for no less than 14 days and no more than 30 days, two to four times a day, depending on the patient's weight and age. The composition is used as a medicine for treatment of the gastrointestinal disorders, including bacterial, viral, protozoal enteric infections, food poisoning, acute and chronic hepatitis and cirrhosis, diarrhea, peptic ulcer, Crohn's disease, ulcerative colitis, irritable bowel syndrome, mineral disorders with Ca/Mg deficiency, including osteoporosis and other alterations of the bone formation, as an immunomodulator in atopic dermatitis and immunodeficiency conditions, for protection and recovery of intestinal flora after antibiotic therapy, chemotherapy, and radiotherapy. The result is accelerated achievement of the effect and the enhanced action on the state of intestinal microbiocenosis as well as increased effectiveness of treatment of hepatitis and liver cirrhosis, elimination of undesired adverse effects in clinical usage, and extension of indications, i.e. the extended spectrum of usage in prevention and treatment.
CN101721525A Plaster for treating carbuncle pain The invention relates to a plaster for treating carbuncle pain, which takes dandelion and honeysuckle as main medicines, is assisted with yellow-corktree bark and borneol for clearing away heat and toxic materials and dissipating the tumours of carbuncle and furuncle, is also provided with angelica, weeping forsythia, myrrh and safflower for dredging the qi and promoting blood circulation and is provided with uniflower swisscentaury, red peony root and dahurian angelica root for dispelling the swelling of the carbuncle, breaking the blood stasis and dispelling the toxicity of malignant boil. Various medicines are combined and refined into a plaster for external pasting to treat inflammation, hard lumps, carbuncle swelling and pyocutaneous diseases, thus directly reaching the focus, which is a shortcut which features simpleness, convenience, safety and immediate effect.
EP2094709B1 Thiazole pyrazolopyrimidines as crf1 receptor antagonists The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.
US20100227877 New camptothecin derivatives and uses thereof The present invention provides two new camptothecin derivatives, which were identified as S,R- and S,S-topotecan lactates, respectively. Both compounds have anticancer activities. Pharmaceutical compositions of the new camptothecin derivatives, and cancer therapies with the new camptothecin derivatives or their pharmaceutical compositions were also provided.
WO2010108314A1 Use of fiber pentose or composition containing fiber pentose in manufacture of foods or medicines for preventing and/or treating acidification in diabetic patient Fiber pentose or a composition containing fiber pentose is used in the manufacture of foods or medicines for preventing and/or treating acidification of the body in diabetic patients. The composition comprises fiber pentose and substances that promote absorption in the body of fiber pentose. The substances that promote absorption of fiber pentose are selected from cellulose, vitamin B1, vitamin B5, vitamin B6, thyroxine, adrenalin, potassium ion, magnesium ion and sodium ion. The fiber pentose is xylose, ribose, arabinose, lyxose, ribulose and/or xylulose. The fiber pentose is prepared by mixing cellulose-containing biomass, water and catalyst, hydrolyzing and then fermenting with yeast. The catalyst is selected from hemicellulose hydrolase, organic acid, inorganic acid or biomimetic catalyst.
CN103638024A Application of penehyclidine hydrochloride in treatment of tiny thromboembolism of pulmonary artery caused by infectious shock The invention discloses application of penehyclidine hydrochloride in treatment of tiny thromboembolism of pulmonary artery caused by an infectious shock. Microcirculation can be effectively improved, tissue perfusion is increased, and especially, the penehyclidine hydrochloride has a significant effect on the tiny thromboembolism of pulmonary artery caused by the infectious shock.
CN101224218B Uses of 8-beta-D glucopyranosyl-4',7-dihydroxy isoflavone The invention discloses an application of 8-Beta-D glucopyanosyl-4, 7-dihydroxy isoflavone in the preparation of medicines for the treatment or prevention of foetus ischemia and anoxia in womb. The invention provides a new method for protecting foetus and preventing miscarriage and treating or preventing the foetus ischemia and anoxia in womb.
US20060073156 Fosfomycin and n-acetylcysteine for the treatment of biofilms caused by escheric ia coli and other pathogens of the urinary tract Pharmaceutical compositions for the treatment of infections by pathogens of the urinary tract and, more particularly, compositions containing fosfomycin optionally associated with N-acetylcysteine.
US20080167384 Adding to food or beverage; all forms of retinitis pigmentosa, night blindness Zeaxanthin is useful for the treatment or prevention of diseases of the peripheral retina, and/or for improvement of peripheral vision.
CN101698101B Medicine composite for treating vaginitis The invention relates to a medicine composite for treating vaginitis, comprising main medicine, matrix, bio-adhesive material, release rate regulator and other additives. The medicine composite for treating vaginitis has special bioadhesive and longer keeping time, reduces medicine leakage, prolongs contact time of medicine and vagina mucosa and ensures curative effect; the composite has special vagina slow release performance and can continuously release medicine for 2-7 days; compared with common preparation, the medicine composite prolongs medicine release time and can reduce medicine application times, thus bringing convenience for patients to apply the medicine. Meanwhile, because the medicine composite has the characteristics of bioadhesive and long efficiency of slow release and has no requirements for medicine application time, thus medicine application can be carried out at any time.
WO2006080398A1 Composition for preparing carbon dioxide preparation for external use The invention is directed to a composition for preparing a carbon dioxide preparation for external use characterized by comprising a substance that produces an acid when being hydrolyzed, a carbonate, a thickening agent and water as essential components, and a composition for preparing a carbon dioxide preparation for external use characterized by comprising the essential components, a gelling agent for forming a gel by a calcium ion, and a calcium salt that is insoluble or sparingly soluble in water. According to the invention, the carbon dioxide preparation for external use, which contains sufficient amount of carbon dioxide, from which the carbon dioxide is absorbed transdermally or transmucosally in a sustained manner, and which has a more potent cosmetic or medicinal effect, can be easily prepared. In addition, the composition for preparing a carbon dioxide preparation for external use with a low production cost can be provided.
US7368575 Chronic inflammation, rheumatoid arthritis, colitis, asthma and psoriasis; solid phase synthetic methods to efficiently construct numerous drug-like libraries When a multi-step process reaction is carried out in a solution, it generally requires several treatments and purification procedures to go through with after the reaction, however, the inventive method for preparing 2,2′-disubstituted-3,4-dihydro-7,8-disubstituted-6-amino benzopyran derivative using a solid-phased synthetic method simplifies the treatment and purification procedures after the reaction, which makes possible to efficiently construct numerous drug-like libraries. In particular, since the inventive method of the present invention comprises the steps of introducing a carbonate linker of formula 2 into Wang resin used as a common solid support (Step 1); synthesizing various benzopyran in a carbamate form of formula 3 as a key intermediate by reacting various amino benzopyran derivatives with the carbamate resin of formula 2 (Step 2); synthesizing 2,2′-disubstituted-3,4-2H-6-substituted benzopyran resin of formula 4 (Step 3); and synthesizing 2,2′-disubstituted-3,4-2H-6-alkylamino benzopyran derivative of formula 1 using a dichloromethane solution containing TFA or an organic solvent containing an organic acid, the inventive method is capable of efficiently synthesizing various 2,2′-disubstituted-3,4-2H-6-alkylamino benzopyran derivatives. Consequently, the present invention has developed a new technique for constructing 2,2′-disubstituted-3,4-2H-6-alkylamino benzopyran library using a solid-phase parallel synthetic method and makes increased the applicability of combinatorial chemical synthetic method. Further, 2,2′-disubstituted-3,4-2H-6-alkylamino benzopyran derivative prepared by the inventive method has a high inhibitory effect to 5-lipoxygenase (5-LO) activity, and therefore, can be effectively used for developing a new propylactic or therapeutic drug for leukotriene activation-related diseases such as chronic inflammation, rheumatic arthritis, colitis, asthma and psoriasis.
CN103191056A Oral liquid preparation of moxifloxacin as well as preparation method and application thereof The invention relates to an oral liquid preparation containing moxifloxacin or salt thereof, a preparation method of the oral liquid preparation, and application of the preparation in treatment of a bacterial infected patient with dysphagia. The preparation is characterized by comprising the following components, based on the moxifloxacin, 0.04 to 4 percent (w/v) of moxifloxacin or salt thereof, and more than 1.0 percent (w/v) of a masking agent. According to the oral liquid preparation, the preparation method and application thereof, the problem of bitter taste of moxifloxacin can be solved, the bitter taste can be successfully masked, and the oral liquid preparation of moxifloxacin which facilitates administration of the patient with dysphagia and is good in taste can be prepared.
WO2010072277A1 Local anesthetic for relieving breast pain The present invention relates to the use of at least one local anesthetic for the prophylactic and/or therapeutic treatment of breast pain, in particular pain caused by medical examinations, especially by mammography, uncomfortable pressure or compression sensations, a decreased sense of well-being or the like, in particular of the female breast.
US20120189616 Isosorbide nitrates The present invention relates to new 3-substituted 6-nitrooxy-hexahydrofuro[3,2-b]furane derivatives possessing a superior pharmacological activity in thrombosis and in coronary ischemia models.
US20120016005 Phagocytic cell delivery of rnai The present invention provides a particulate delivery system for delivering an RNAi construct to phagocytic cells such as macrophages, comprising various configurations of a complex comprising a phagocytic cell-targeting moiety and an RNAi construct. The invention further provides methods of making the delivery system, and their uses, such as treating phagocytic cell-associated disease conditions.
US8318779 Lysine related derivatives as HIV aspartyl protease inhibitors The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
US20080319034 Method for producing precious material for ornamental articles and precious material for ornamental articles which can be obtained in particular by means of this method Method for producing a precious material for ornamental articles, which envisages introducing, into the plasticization chamber of an extruder at a temperature of between 120 and 220° C., an amount of a Polymer composition and an amount of a metallic powder formed with one or more precious metals having particles with an average size of less than 0.5 micron in order to achieve thorough mixing between the amount of polymer composition in the liquid state and the amount of metallic powder by means of one or more screws provided with mixing segments; and then an extrusion and cutting step in order to obtain an intermediate product with a precious metal content to be treated during a subsequent forming step aimed at obtaining an ornamental article in the desired form.
US8119116 Therapeutics for cancer using 3-bromopyruvate and other selective inhibitors of ATP production The present invention relates to methods of treating a cancerous tumor using selective inhibitors of ATP production. The present invention also relates to pharmaceutical preparations comprising such inhibitors and methods for administering them intraarterially directly to a tumor, as well as methods for identifying compositions that selectively inhibitor ATP production for use in the invention.
CN103432081A Method for compounding drug-containing pellet core of metformin hydrochloride controlled-release pellet preparation The invention provides a method for compounding a drug-containing pellet core of a metformin hydrochloride controlled-release pellet preparation. The drug-containing pellet core comprises the following components according to weight percentages: 40.0%-70.0% of metformin hydrochloride, 25.0%-55.0% of a filler and 0.4%-5.0% of a binder, and the sum of the weight percentages of all the components is 100%. The compound metformin hydrochloride-pioglitazone hydrochloride controlled-release pellet preparation, which is formed by mixing the drug-containing pellet core with other medicinal materials, has an ideal effect of regulating blood sugar level, is capable of reducing the toxic and side effects of drugs and achieving a continuous and stable blood sugar level reduction effect in vivo, is advantageous for improving the compliance of a patient, has high bioavailability and stable blood concentration, and is capable of effectively improving the clinical curative effect, and therefore, good dosage regimens and curative effects are provided for domestic and overseas diabetics.
EP1121941B1 Sorbefacients and preparations for percutaneous absorption containing the same Percutaneous sorbefacients comprising hexylene glycol and l-menthol, more particularly, percutaneous sorbefacients for female hormones or derivatives thereof; and preparations for percutaneous absorption which comprise a styrene/isoprene/styrene block copolymer and/or polyisobutylene, a softener and a tackifier as the base components, hormones, in particular, follicle hormone and/or luteal hormone as the drug component and hexylene glycol and l-menthol as a sorbefacient.
US7186401 comprises magnesium stearate for improved storage stability; inhalers The aim of the invention is to improve the moisture resistance of dry powder formulations for inhalation which contain a pharmaceutically ineffective carrier of not-inhalable particle size and a finely divided pharmaceutically active compound of inhalable particle size and to also improve the storage stability of said formulations. To this end, magnesium stearate is used in said formulations. One of the features of the inventive dry powder is that a high fine particle dosage or fine particle fraction can be maintained also under relatively extreme temperature and humidity conditions.
WO2009049105A2 Methods for inducing satiation One aspect of the present invention relates to methods for inducing satiation to prevent or treat obesity and manage weight/body composition by decreasing food intake both during a meal and to increasing the duration of time between meals. Specifically methods to increase the size of a food bolus without increasing the corresponding energy density are disclosed. In addition, methods of inducing satiation through small intestine volume displacement and placement of pressure on the walls of the small intestine in a manner which is non-invasive and does not result in significant pain or discomfort are disclosed.
CN102755477A Externally-used plaster for treating onychomycosis The invention discloses an externally-used plaster for treating onychomycosis. The externally-used plaster for treating the onychomycosis is characterized by comprising the following raw materials in part by weight: 10-12 parts of natural indigo, 10-12 parts of dried alum, 15-18 parts of realgar, 10-12 parts of dandelion, 10-12 parts of cortex lycii radicis, 18-20 parts of pseudolarix, 15-18 parts of snake slough, 10-12 parts of stiff silkworm, 10-12 parts of rhizoma arisaematis, 18-20 parts of saponin, 10-12 parts of unprocessed radix aconiti, 15-18 parts of castor bean, 15-18 parts of wind fairy, 18-20 parts of radix sophorae flavescentis, 30-50 parts of vaseline, 15-18 parts of semen momordicae, 15-18 parts of impatiens balsamina and 400-700 parts of glacial acetic acid. The externally-used plaster for treating the onychomycosis is good in therapeutic effect, short in course of treatment, small in side effect and convenient to use.
US20100261769 Topical Compositions Comprising Non-Proteogenic Amino Acids and Methods of Treating Skin Cosmetic compositions comprising non-natural, non-proteogenic amino acids and methods of using such compositions to impart antiaging benefits to the skin are disclosed. The non-natural, non-proteogenic amino acids are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging, and in particular, are enhancers of LOXL-1.
WO2008039987A2 Methods of treating pulmonary distress Provided is a method of increasing the forced expiratory volume in one second (FEV1) in a subject comprising administering to the subject in need thereof a therapeutically effective amount of a liposomal formulation. In some embodiments, the liposomal formulation comprises empty liposomes. Also provided is a method of increasing FEV1 in a subject consisting essentially of administering to the subject a therapeutically effective amount of empty liposomes and pharmaceutical carrier. Additionally, provided is a method of treating cystic fibrosis in a subject comprising administering to the subject a therapeutically effective amount of empty liposomes.
EP1276463B1 Hemostatic agent, method and carrier for applying a blood clotting agent A hemostatic agent, method and carrier for arresting the flow of blood and other protein containing body fluids flowing from an open wound and for promoting wound healing. A broad aspect is directed to a substantially anhydrous admixture of an oxyacid salt and a hydrophilic proton donor which will hydrate in the presence of blood and body fluid to produce cations to promote blood clotting. The preferred oxyacid salts are alkali and alkaline earth salts of transition metals and halogen oxyacids with oxidizing capabilities sufficient to accelerate blood clotting. Another embodiment of the invention includes the compound containing an oxysalt plus a hydrophilic polymer such as carboxy methylcellulose, polyvinyl, alcohol, an alginate, and all soluble gums. Still another embodiment of the invention includes the compound formed of an oxyacid salt in combination with a hydrophilic proton donor and a solid desiccant which further accelerates blood coagulation reaction rates. The cation exchange material or an admixture of an alkali metal oxyacid salt plus acidic inorganic salt produces a scab or protective coating over the wound for protection and enhanced healing. Oxygen produced during the reaction substantially reduces the level of bacteria, virus and fungus at the wound. The resin is performance-enhanced for greater fluid uptake and more rapid coagulation.
US20080070950 Amorphous rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2- methylpropionic acid and its pharmaceutical compositions The present invention provides an amorphous form of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid. This invention also provides processes for preparing the amorphous form and pharmaceutical compositions including the amorphous form.
CN101306072A Gadol buccal tablet and its preparation method The invention provides a rhodiola root buccal tablet, which is prepared from rhodiola root extract dry powder, mannitol, dextrin, CMC-NA, a sweetening agent, micropowder silica gel, magnesium stearate, menthol and lemon extract. The invention further provides a method for preparing the rhodiola root buccal tablet. The buccal tablet provided by the invention is health food prepared from the main raw material of rhodiola root extract dry powder. Proven through animal meal function test, the buccal tablet has the health protection functions of easing strain of human bodies, and improving tolerance to anoxia. The buccal tablet is prepared by adopting the advanced process, and has the special aroma of rhodiola root and moderate aftertaste, which is sweet and tasty without bitter. The tablet can be conveniently administrated by the young, the middle-aged and the elderly.
US20100081695 2-N-{5-[ [4-[2-(methyl-2-pyridinylamino) ethoxy] phenyl]methyl]-2,4-thiazolidinedione) butanedioic acid, methods of preparation and compositions with rosiglitazone maleate Disclosed is an isolated compound of the formula: along with methods of detecting it and of minimizing it in improved pharmaceutical compositions of rosiglitazone maleate.
US7081254 For relieving or improving skin roughness and suppressing wrinkling, shows neither any offensive smell nor stickiness, gives users a dry feel upon use, and exhibits controlled foaming upon production and stability The invention relates to a skin preparation for external use, which contains a lamellar structure containing a fatty acid monoglyceride as a main component, and vitamin A or a derivative thereof. The skin preparation for external use has high effects of improving skin roughness and suppressing wrinkling, etc., shows neither any offensive smell nor stickiness, and exhibits controlled foaming upon the production thereof.
WO2013077553A1 Composition for alleviating hypoglycemia The present invention relates to a biopharmaceutical composition or a food composition in a solution formulation, wherein the composition includes 40-90 wt% of glucose and 10-60 wt% of water but excludes preservatives. The composition for alleviating hypoglycemia shows extraordinary long-term shelf-life even without preservatives. Since the composition is in a solution formulation, the composition can be easily ingested and rapidly absorbed by the human body. Also, the composition can rapidly increase blood glucose levels, and is thus highly effective at alleviating hypoglycemia.
US20080221205 effect on bone proliferation with the side effect reduced; degenerative bone disease and rheumatoid arthritis The present invention relates to furan derivatives and pharmaceutical compositions containing them to prevent and cure osteoporosis. The furan derivatives of the present invention have effect on bone proliferation with the side effect reduced, so that they can be used for bone disease.
EP1446127B1 Triazepine derivatives as neurotrophic agents This invention relates to a series of triazepines of Formula I and II, and pharmaceutical compositions containing them. The compounds of the invention have neurotrophic activity and are useful in the treatment and prevention of neuronal disorders such as Parkinson's disease, Alzheimer's disease, stroke, multiple sclerosis, amyotrophic lateral sclerosis diabetic neuropathy and Bell's palsy.
WO2005100337A1 Substituted dioxolane derivatives and their use of preparing the neuroregulator The present invention relates to the dioxolane derivatives of general formula (I), which have nerve nutrition effects, or to the pharmaceutical acceptable salts or hydrate thereof. Each group of general formula (I) is defined as the specification. The present invention also relates to the pharmaceutical composition comprising the mentioned compounds, and the use of the pharmaceutical composition as FK506 binding protease activity inhibitor to prepare the medicines which can prevent or treat the neurodegenerative diseases and other neurological disorders caused by nerve damage or related diseases.
US20050124557 Use of benzothiazepines having activity as inhibitors of ileal bile acid transport for reducing cholesterololemia The use of an ileal bile acid transport (IBAT) inhibitor and the use of a combination of an IBAT inhibitor and an HMG CoA reductase inhibitor in the treatment of a warm-blooded animal, such as man, with hypercholesterolemia and/or other forms of dyslipidaemia wherein said hypercholesterolemia and dyslipidaemias are characterized by defects in lipoproteins or their receptors is described.
US20110172141 Process for preparing microparticles A process for preparing microparticles comprising a biologically active material and a polymer and having a mean particle size expressed as the volume mean diameter (VMD) of from 10 to 500 μm, wherein the biologically active material is substantially insoluble in the polymer, which process comprises: a. contacting a mixture of the biologically active material or a precursor thereof, the polymer or a precursor thereof and a processing aid with a supercritical fluid which is capable of swelling the polymer under temperature and pressure conditions necessary to maintain the fluid in a supercritical state; b. allowing the supercritical fluid to penetrate and liquefy the polymer, whilst maintaining the temperature and pressure conditions so that the fluid is maintained in a supercritical state; c. releasing the pressure to precipitate microparticles comprising the biologically active agent and the polymer.
CN101837075A Composition for preventing and treating dementia The invention relates to application of a Lycoris aurea extract and/or an organic solvent extract of the Lycoris aurea extract and/or lycoricidine and lycoricidinol obtained by separating the extract or the organic solvent extract in preparing a composition for preventing and treating dementia.
US7358242 N-benzyl-2-[4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-2,3,6,10b-tetraaza-benzo[e]azulen-6-yl]-N-isopropyl-acetamide; cholecystokinin-A (CCK-A) receptor agonist; antidiabetic; obesity This invention relates to CCK-A agonists of Formula (I) wherein R1-R4, A, B, X, D, E and G are as defined in the specification, as well as, among other things, pharmaceutical compositions containing the compounds and methods of use of the compounds and compositions. The compounds are useful in treating diabetes.
WO2005121126A1 Polycyclic pyrazines as potassium ion channel modulators The present invention provides a genus of polycyclic pyrazines of formula I (I) that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods; wherein A and B are independently substituted or unsubstituted 5- or 6-membered heterocycloalkyl, or substituted or unsubstituted 5- or 6- membered heteroaryl, W1 is formula II (II); W2 is -CH=, -NH-, -N=, -S-, or -O-; Z1 is formula III (III) or formula IV (IV); Z2 is -CH=, -NH-, -N=, -S-, or -O-; Y is a bond, -CH=N-NH-, -NH-CH2-, or -NR5-; s and t are independently integers from 1 to 4; R1, R2A, R2B and R3 are independently or unsubstituted alkyle, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted 3- to 7- membered cycloalkyl,, substituted or unsubstituted 5- to 7-membered heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and R5 is H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted 3- to 7- membered cycloalkyl,, substituted or unsubstituted 5- to 7-membered heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; wherein if s is greater than one, then each R1 is optionally different; wherein if t is greater than on, then each R3 is optionally different; wherein two R1 groups are optionally joined together with the atoms to which they are attached to form a substituted or unsubstituted ring; and wherein two R3 groups are optionally joined together with the atoms to which they are attached to form a susbtituted or unsubstituted ring.
WO2008088617A1 Treatment of copd The present invention provides methods for treating chronic obstructive pulmonary disease. In some embodiments of the invention, methods for treating COPD comprise administering PGI2 or a prostacyclin analog to a subject in need of such treatment.
WO2014100231A1 Use of cannabinoids and terpenes for treatment of organophosphate and carbamate toxicity Pharmaceutical compositions in which isolated cannabinoid receptor modulators are optionally combined with terpene blends in a pharmaceutically acceptable carrier. Methods for treating or preventing a disease, disorder, dysfunction or condition caused by exposure to an organophosphate or carbamate acetylcholineesterase inhibitor with the inventive compositions are also disclosed.
WO2011100838A9 Derivatives of l-plienyl-1.5-diliydio-benzo[b] [1.4]diazepine-2.4-dione as inhibitors of hiv replication Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.
CN102429912A Pharmaceutical composition prepared with micronized prasterone or sodium prasterone sulfate and use thereof The invention relates to a pharmaceutical composition prepared with micronized prasterone or sodium prasterone sulfate and a use thereof. The pharmaceutical composition comprises the following pharmaceutical ingredients: the micronized prasterone or the sodium prasterone sulfate, wherein the granulation size is 1 micron to 120 microns, preferably normal distribution of 1 micron to 50 microns, further preferably normal distribution of 10 microns. The content of the pharmaceutical ingredient is 10 mg-200 mg, preferably 25 mg-100 mg. The pharmaceutical ingredients can be prepared as the product in any pharmaceutically acceptable dosage form. The invention further provides the use of the pharmaceutical composition in preparing the drugs for treating and/or preventing sexual dysfunction, osteoporosis, lupus erythematosus, aesthetic dermatology, postpone senility and woman urogenital atrophy syndrome.
CN103610637A Rifampicin injection and preparation method thereof The present invention relates to a rifampicin injection, which is prepared from the following materials: 20 g of rifampicin, 12 g of tartaric acid, 10 g of sorbic acid, 55 g of polyethylene glycol 400, and 2000 ml of water for injection, wherein the pH value is adjusted to 6.3-6.5.
USRE39606 Synthetic libraries of random oligomers, each member comprising an oligomer linked to a microchip encoded with information identifying structure of oligomer, for drug screening The present invention provides labeled synthetic libraries of random oligomers and methods and apparatus for generating labeled synthetic oligomer libraries. Each member of such a library is labeled with a unique identifier tag that specifies the structure or sequence of the oligomer. In a preferred embodiment of the present invention the identifier tag is a microchip that is pre-encoded or encodable with information that is related back to a detector when the identifier tag is pulsed with electromagnetic radiation.
WO2014079377A1 Antitumor prodrugs with function of p-glycoprotein inhibition Antitumor prodrugs with function of P-glycoprotein inhibition are disclosed. The prodrugs are amphiphilic substances composing of antitumor drug covalently linked with polyethylene glycol succinate with function of P-glycoprotein inhibition via a linker. The linker has a sensitive bond and two reactive groups separately covalently linked with antitumor drug and polyethylene glycol succinate. The sensitive bond is a scissile chemical bond in the intracelluar reducing environment or acidic environment of tumor cells.
CN102229606A 2-methylbenzofuran derivative containing isoxazole heterocycle, and preparation method and application thereof The invention discloses a 2-methylbenzofuran derivative containing isoxazole heterocycle shown as formula (I), wherein, in formula (I), R1 represents a substituted phenyl; R2 and R4 individually represent benzoyl or substituted benzoyl; and R3 represents H, hydroxy, halogen, nitryl or C1-C3 alkyl. The invention has beneficial effects that (1) a new 2-methylbenzofuran derivative containing isoxazole heterocycle is provided; (2) the compound can substantially inhibit monoamine oxidase activity and provide researching foundations for screening of new antidepressant and Parkinson-resistant medicaments; (3) the preparation method is easy to realize automatic operation to accelerate synthesis process and increase efficiency, and recycle of raw materials can be realized; (4) a synthesis technology of the compound of the invention is convenient for operation, and is apt to be applied to new compound synthesis through a high-throughput compound screening.
WO2010133970A1 Targeting micrornas for metabolic disorders Provided herein are methods and compositions for the treatment of metabolic disorders. Also provided herein are methods and compositions for the reduction of blood glucose level, the reduction of gluceoneogenesis, the improvement of insulin resistance and the reduction of plasma cholesterol level. In certain embodiments, the methods comprise inhibiting the activity of miR-103. In certain embodiments, the methods comprise inhibiting the activity of miR-107. In certain embodiments, the activity of both miR-103 and miR-107 is inhibited. In certain embodiments, such methods comprise administering a compound comprising an oligonucleotide targeted to a microRNA.
EP2490533A1 Novel compositions for preventing and/or treating lysosomal storage disorders The present invention provides novel compositions as well as methods for preventing and/or treating lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.
CN1857200A Medicinel liquid containing proton pump inhibitor The present invention provides a kind of liquid medicine containing proton pump inhibitor and its preparation process and application in preparing injection. The liquid medicine contains proton pump inhibitor medicine with pharmaceutical activity and in effective treating amount and one or several pharmaceutically acceptable short chain alcohol solvent. The liquid medicine as one new preparation form of proton pump inhibitor medicine has high stability.
CN101912365A Sulbenicillin sodium powder injection and preparation process thereof The invention provides sulbenicillin sodium powder injection and a preparation process thereof. The sulbenicillin sodium in the powder injection is a sulbenicillin sodium crystalline hydrate and the chemical formula of the sulbenicillin sodium is C16H16N2Na2O7S2.H2O. The powder injection is obtained through refrigerating and drying processes. The refrigerating process comprises the following steps of: putting sub-packaged solution of sulbenicillin into a freeze-drying tank; cooling the solution to 27 to 35 DEG C below zero at the speed of between 25 and 35 DEG C/min; preserving heat for 0.5 to 1 hour; raising the temperature to 15 to 10 DEG C below zero; preserving heat for 0.5 to 1 hour; slowly reducing the temperature to 50 to 45 DEG C below zero; preserving heat and refrigerating for 2 to 3 hours; and subliming and drying to obtain the powder injection. The obtained sulbenicillin sodium has the advantages of low moisture absorption capacity, high stability and convenient transportation and storage.
US20050159426 Novartis drug called Imatinib, 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, methanosulfonate; synergistic mixture with a second antineoplastic agent 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide or a pharmaceutical acceptable salt thereof can be used in the treatment of neuroblastoma. The invention also relates to a combination of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide or a pharmaceutical acceptable salt thereof with one or more antineoplastic agents.
EP1392270B1 Abuse resistant pharmaceutical composition containing capsaicin A pharmaceutical composition intended for oral use contains the effective ingredient(s), capsaicin, and other typical fillers and excipients. The composition is preferably in the form of a solid oral dosage form. Transdermally administered compositions are also within the purview of the invention. Aside from the effective pharmaceutical ingredient(s) the composition includes an amount of capsaicin which serves as a deterrent to the intranasal, intravenous, or oral abuse of the composition. Such a composition deters abusers from crushing prescription pharmaceutical tablets for abusive snorting, injection, or ingestion.
CN102872123A Application of Houttuynoid C in medicament for treating bladder cancer The invention discloses application of Houttuynoid C in preparing a medicament for treating bladder cancer, and belongs to the technical field of new use of medicaments. Houttuynoid C is found to have obvious inbibitional effect on the growth of human bladder cancer cell line T-24 through MTT (Methyl Thiazolyl Ternzolinm) anticancer activity evaluation in vitro. Therefore, Houttuynoid C can be used for preparing the anti-bladder cancer medicament and has excellent prospects in development and application. The use of Houttuynoid C in preparing the medicament for treating the bladder cancer involved in the invention is disclosed for the first time; and the framework type of Houttuynoid C is a brand new framework type and Houttuynoid C has an unexpectedly high inhibition activity for bladdercancer cells.
CN101032494A Application of Asiatic Acid in the preparing of medicine for preventing and curing kidney fibrosis The present invention discloses the application of asiatic acid in preparing medicine for preventing and treating kidney fibrosis. By means of the effect of asiatic acid on kidney fibrosis of rat, the present invention proves the effect of asiatic acid in antagonizing kidney fibrosis. Therefore, asiatic acid may be used as the active component for medicine to treat kidney fibrosis.
WO2008106536A1 Use of silodosin in a once daily administration for treating benign prostatic hyperplasia Patients having symptoms associated with benign prostatic hyperplasia can be treated with a once daily composition containing silodosin or a pharmaceutically acceptable salt thereof.
US20110124739 Use of Sphingosine-1-phosphate (S1P) Receptor Agonists for the Treatment of Brain Degenerative Diseases Disclosed is the use of sphingosine-1-phosphate (S1P) receptor agonists, preferably 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol, in the treatment of progressive dementia or brain degenerative diseases
CN101152456B Medicine for treating hyperosteogeny, rheumatic arthritis and prolapse of intervertebral disc The present invention discloses a medicine for curing bone fracture and the medicine is a medicine combination made of raw materials of pure natural plant, animal and mines with a process; at the sametime, the present invention also discloses the preparation method of the medicine combination; the raw materials for making the medicine are easy to get and the preparation method is simple.
WO2005115405A8 Methods for treating or preventing restenosis and other vascular proliferative disorders Described herein is the use of ribonucleotide reductase inhibitors in the prevention or treatment of restenosis and other vascular proliferative disorders.
CN1923178A Oleanolic acid liposome preparation, freeze dried powder injecta thereof and its preparation The invention relates to the liposome with oleanolic acid, relative freeze dried. Wherein, the liposome comprises oleanolic acid, phosphatide, cholesterol and surface activator, while their ratios are 1:10-80:0-20:0-50; the freeze dried is formed by oleanolic acid agent, dextran, monosaccharide, diose and/or polysaccharide, while their amounts are based on the mass of phosphatide, that one deal of phosphatide takes 0.2-5.0 deals of them; when the oleanolic acid is made into liposome, it can be inactively targeted into liver, to improve the drug density and reduce side effect; the drug will be slowly released in human body, to prolong the effective time; and its package rate is higher than 75%, particle diameter is 100-800cm.
CN103417843A Method for preparing colon-cleansing particles used before gynecological surgery The invention discloses a method for preparing colon-cleansing particles used before gynecological surgery and aims to solve the treatment problem before gynecological surgery. The method is characterized in that the colon-cleansing particles are prepared by the following active pharmaceutical ingredients: by weight proportion, horseweed herb, fructus cinnamomi, radix ranunculi ternati, Chinese starjasmine stem, herbof denseflower bulbophyllum, rhizoma polygonati, dipsacus roots, tangerine peel, sunflower flowers, turbo cornutus solander, amblystegium serpens and magnesium sulfate. The method includes the following steps: (1), extracting volatile oil from dipsacus roots, fructus cinnamomi and herbof denseflower bulbophyllum coarse powder for standby use; (2), smashing turbo cornutus solander and amblystegium serpens into fine powder for standby use; (3), adding water in horseweed herb, radix ranunculi ternati, Chinese starjasmine stem, rhizoma polygonati, sunflower flowers and tangerine peel for decoction twice, filtering, combining filtrate, concentrating the filtrate, adding ethanol for deposition, taking supernate, recycling ethanol and concentrating to obtain thick paste; (4), adding the volatile oil obtained in step 1 and the fine powder and magnesium sulfate obtained in step 2 in the thick paste obtained in step 3, uniformly stirring, forming particles, drying and obtaining the colon-cleansing particles. Clinical experiments show that the colon-cleansing particles have good colon-cleansing effect when used before gynecological surgery, and the colon-cleansing particles are worthy of clinical popularization and application.
EP1711507B1 Crystalline form of risedronate monosodium Crystalline monosodium salt of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid, having the X-ray pattern with characteristic interplanar distances 4.35; 8.44; 13.42 and 15.73 ú.
CN103169652A Veterinary alkaline lincomycin injection as well as preparation method and use thereof The invention provides veterinary alkaline lincomycin injection. The veterinary alkaline lincomycin injection is injection which is prepared by using lincomycin hydrochloride as the material, and adding alkali to adjust the pH value of the injection to 9.0-11.5. The invention further provides a preparation method of the injection and a use of the injection. The alkaline lincomycin injection provided by the invention can be used for effectively improving the utilization rate of the lincomycin, so that the treatment effect is remarkably better than that of the lincomycin hydrochloride injection, the preparation stability is good, the quality is controllable and the application value is high.
US20110237589 Guanidine compounds, and use thereof as binding partners for 5-ht5 receptors The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
US20090053283 such as vulvodynia via comprising administering polyarginine; for treatment and/or prevention of glaucoma, pulmonary hypertension, asthma, chronic obstructive pulmonary disease, erectile dysfunction, Raynaud's syndrome, heparin overdose, vulvodynia, and wound healing agents This invention relates to compositions and methods for treatment of vascular conditions. The invention provides arginine polymers and arginine homopolymers for the treatment and/or prevention of glaucoma, pulmonary hypertension, asthma, chronic obstructive pulmonary disease, erectile dysfunction, Raynaud's syndrome, heparin overdose, vulvodynia, and wound healing. The invention also provides arginine polymers and arginine homopolymers for use in organ perfusate and preservation solutions.
CN103536623A Potassium magnesium aspartate composition freeze-dried powder for injection The invention provides a potassium magnesium aspartate composition freeze-dried powder for injection, and belongs to the field of medicine and medicine preparation technology. The potassium magnesium aspartate composition freeze-dried powder comprises following raw material ingredients, by weight, 850 to 1700 parts of potassium magnesium aspartate, 164 to 328 parts of potassium hydroxide, 70 to 140 parts of magnesium oxide, 500 to 1000 parts of chitosan nanoparticle, and 4000 to 8000 parts of injection water. Advantages of the potassium magnesium aspartate composition freeze-dried powder are that: the potassium magnesium aspartate composition is made into freeze-dried powder for convenience in clinical application; the potassium magnesium aspartate composition is capable of prolonging medicine half-life period significantly, prolonging medicine action time, increasing medicine bioavailability, and reducing medicine use numbers of patient; the potassium magnesium aspartate composition freeze-dried powder injection is stable in properties, is convenient for carrying and transporting, and is capable of reducing dosage of the auxiliary materials, improving solubility of the main medicine ingredient, and ensuring clinical medication safety.
US20110112048 Use of beta-glucan on upper respiratory tract infection symptoms and psychological well-being Studies involving placebo-controlled, double-blinded designs to evaluate the effect of beta-glucan compositions on upper-respiratory tract infections and psychological wellness were carried out. During the course of the reporting periods of these studies, subjects in the treatment groups reported fewer URTI symptoms, better overall health and a more positive psychological assessment based on a POMS survey.
EP2311461A1 Methods for treating cancer by inhibiting mitosis using pyrrolo[2,3-d]pyrimidines A compound having the following formula: wherein X is selected from the group consisting of a C1 to C6 alkyl group, a heteroalkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, an arylalkyl group, and a heteroarylalkyl group; wherein R1 is selected from the group consisting of hydrogen, a C1 to C6 alkyl group, a heteroalkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, an arylalkyl group, and a heteroalkyl group; wherein R2 is selected from the group consisting of hydrogen, a C1 to C6 alkyl group, a plurality of C1 to C6 alkyl groups, a heteroalkyl group, a plurality of heteroalkyl groups, an alkoxy group, a plurality of alkoxy groups, a substituted or unsubstituted aryl group, a plurality of substituted or unsubstituted aryl groups, a substituted or unsubstituted heteroaryl group, and a plurality of substituted or unsubstituted heteroaryl groups; wherein R3 is selected from the group consisting of zero, a C1 to C6 alkyl group, a heteroalkyl group, an alkenyl group, and a heteroalkenyl group; and wherein R4 is selected from the group consisting of a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, an arylalkyl group, a heteroarylalkyl group, and hydrogen, and R4 is hydrogen when R3 is zero, for use in a method of treating cancer by inhibiting mitosis, wherein said cancer is optionally one selected from: melanoma, leukemia, colon cancer, prostate cancer, lung cancer, pancreatic cancer, ovarian cancer, renal cancer, breast cancer, brain cancer, and Kaposi's sarcoma cancer.
US20100075986 Oxophenyl-Cyclohexyl-Propanolamine Derivatives, Production And Use Thereof In Therapeutics The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally substituted, R2 represents H, a halogen atom, an —S(O)zR3, —NHSO2R3, —NHSO2-phenyl or —NHSO2—(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where R3 represents a (C1-C4)alkyl group, said phenyl being optionally substituted; A is chosen from where n is equal to 0, 1 or 2, R4 and R5 represent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, —CONH2, —CO-phenyl, —COOR3, —CH(phenyl) (OH) and —C(phenyl)2(OH) group, or R4 and R5 form together an optionally substituted 6-membered aromatic ring, R6 represents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.
CN1883542A Medicament with borneol and borax for treating rhinitis The invention discloses a medicament for treating chronic simple rhinitis and chronic hypertrophic rhinitis, which is prepared mainly from orpiment, sulfur, bornyl alcohol, mercurous chloride, Chinese honey locust and borax. The invention also discloses the process for preparing the medicament.
CN101559055A Application of medicine The invention discloses paroxetine and new application of officinal salts thereof. The paroxetine is characterized in that the paroxetine and officinal salts thereof are applied to the preparation of a medicine treating reproductive system disease comprising inflammation, frigidity, premature ejaculation, and the like. Pharmacological experiments and clinical experiments show that the paroxetine has the advantages of small side effect, wide therapeutic window, and the like, a patient can not generate an after effect after taking the paroxetine, and the paroxetine has the characteristic of new application of an old medicine; and the paroxetine has favorable pharmacological effect.
CN101574415A Patch for preventing and treating external infection The invention discloses a patch for preventing and treating external infection, belonging to a medicine preparation with tablet-shaped base materials as characteristics or pertaining to the technical field of transdermal drug delivery preparation, particularly relates to a patch for preventing and treating external infection by using a mode of treating internal disease with external therapy. The ointment of the patch consists of angelica, herba schizonepetae, clematis chinensis, burdock, native copper, glutin, borneol and camphor. The patch can be prepared by the steps of: crushing the angelica, herba schizonepetae, clematis chinensis, burdock, native copper, borneol and camphor into medicinal powder, putting the medicinal powder of the medicaments into hot melt glutin in sequence according to technical requirements, evenly stirring to prepare the ointment, and finally coating the ointment on a back lining layer for obtaining the patch. The patch uses a small amount of medicaments but has obvious therapeutic effectiveness and is applicable to the treatment of external infection of various symptoms. The use of the patch is convenient, so that the patients not only can use the patch by self-determination but also can stop using the patch at any time. Without irritating skin, the patch is easily accepted by most of patients.
CN101953828B Application of angle flavonoids lignan to preparation of medicaments for treating viral hepatitis B The invention relates to application of an angle flavonoids lignan to preparation of medicaments for treating viral hepatitis B, in particular to application of the angle flavonoids lignan or medicinal salts thereof to preparation of medicaments for inhibiting hepatisis B virus (HBV) DNA replication and treating HBV infection diseases. The flavonoids lignan can exactly inhibit HBV DNA activity; the inhibition activity of the flavonoids lignan with high dosage (20 microgram/ml) to the HBV DNA replication is 189 percent higher than that of alpha-interferon with the maximum concentration of 10,000 unit/ml; and the flavonoids lignan belongs to a strong-effect non-nucleosides inhibition HBV natural product. The pharmacological results show that the angle flavonoids lignan or the medicinal salts thereof can be expected to be used for preparing the medicaments for inhibiting hepatisis B virus (HBV) DNA replication and treating the HBV infection diseases.
CA2380455C 9a-azalides with antibacterial activity Compounds of formula (I), formula (II), formula (III), and formula (IV) or pharmaceutically acceptable salts or prodrugs thereof, are antibacterial agents. Compositions containing the compounds, processes for making the compounds, synthetic intermediates employed in the processes, and methods for treatment and prevention of bacterial infections are disclosed.
US20100210580 Vitamin B12 Nasal Spray and Method of Use The present invention relates generally to vitamin B12 nasal spray compositions and methods of using the same in the treatment of vitamin B12 deficiency and various disorders that are related to such deficiency. In particular embodiments, the present invention is directed to treatment methods comprising intranasal administration of a cobalamin composition according to a particular dosing and frequency schedule and to a preservative-free nasal spray composition comprising a cobalamin compound useful in the practice of such treatment methods.
US7060834 Using a 2-aminoquinoline compound Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R1, b, R4, R5, R6, R7 and R8 are any of a number of groups as defined in the specification, and pharmaceutical compositions and methods of treatment utilizing such compounds.
WO2014111811A1 Veterinary supplements Veterinary supplements comprising one or more Nrf2-activating agents are disclosed. The veterinary supplements may further comprise omega-3 fatty acids and collagen. The veterinary supplements are effective for treating, inhibiting, reducing and/or preventing oxidative stress.
WO2006123550A1 Prophylactic or therapeutic agent for inflammatory disease [PROBLEMS] To provide a therapeutic agent for an inflammatory disease which has an anti-inflammatory effect, an anti-allergic effect and an immunosuppressive effect. [MEANS FOR SOLVING PROBLEMS] A prophylactic or therapeutic agent for an inflammatory disease which comprises 6,9,12,15-hexadecatetraenoic acid or a pharmaceutically acceptable salt or ester thereof as the active ingredient. The pharmaceutically acceptable salt of 6,9,12,15-hexadecatetraenoic acid is, for example, a sodium, potassium, magnesium, calcium, ammonium, pyridine or triethylamine salt of 6,9,12,15-hexadecatetraenoic acid. The pharmaceutically acceptable ester of 6,9,12,15-hexadecatetraenoic acid is, for example, a triglyceride, diglyceride or monoglyceride having 6,9,12,15-hexadecatetraenoic acid as the constituent fatty acid thereof or a lower alcohol ester of 6,9,12,15-hexadecatetraenoic acid.
CN101822662A Application of 9,10-dioxystearic acid (DHSA) in preparing medicaments for preventing and treating diabetes The invention discloses new application of 9,10-dioxystearic acid (DHSA), in particular to application in preparing medicaments for preventing and treating diabetes and provides new application of DHSA. The DHSA can effectively reduce the blood sugar content and improve the insulin sensitivity and has extremely high application prospect in treating type-2 diabetes and obesity. Because the DHSA has the dual actions of reducing the blood sugar and the weight and prepared medicaments are oral preparations, the DHSA not only can be expected to treat the obesity, but also can be expected to treat the diabetes. Because the morbidities of the obesity and the diabetes increase, patients suffering from the two diseases also continuously increase, thus if the DHSA is applied to the treatment of the type-2 diabetes and the obesity, the DHSA can have dual social benefits and economic benefits.
US6846824 E.g., ethyl 3-(4-(2-(3-oxo-2H-1,4-benzoxazin-4-yl)ethoxy)-phenyl-2-ethoxypropenoate where 1,4-benzothiazine or quinoxaline can be substituted for the benzoxazine ring; anticholesterol, diabetic agents; obesity; hyperlimpidemia Compounds of formula (I) its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates can be used to prevent or treat diabetes caused by insulin resistance or impaired glucose tolerance or complications of diabetes caused by insulin resistance or impaired glucose tolerance. The compounds can also be used to reduce cholesterol, body weight, blood glucose, triglycerides and free fatty acids in the blood.
US20100022641 Solid forms of selective androgen receptor modulators The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.
US7081461 Quinazoline compounds and pharmaceutical compositions containing them The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, NH or NR8 where R8 is hydrogen or C1-6alkyl; Ra is a 3-quinoline group or a group of sub-formula (i) where R5, R6 and R7 are various specific organic groups, in the preparation of a medicament for use in the inhibtion of aurora 2 kinase. Novel compounds of formula (I) and pharmaceutical compositions useful in the treatment of cancer are also described and claimed.
CN103083196A Synergistically active ternary anti-microbial mixtures The present invention relates to a synergistically active ternary anti-microbial mixture which comprises 2-phenoxyethanol and at least two different alkanediol comprising 1,2-decanediol, 1,2-octanediol, 1,2-hexanediol or 1,2-pentanediol. The invention further relates to the use of 2-phenoxyethanol for synergistically enhancing the antimicrobial efficacy of mixtures of at least two of the abovementioned alkanediols, a method for preservation or antimicrobial treatment of a perishable product, a method for the cosmetic treatment of certain microorganisms, as well as the use of an inventive mixture of therapeutic treatment of certain microorganisms.
CN101933911A Soft capsule composition for treating senile dementia and preparation method thereof The invention discloses a soft capsule composition for treating senile dementia and a preparation method thereof, in particular a soft capsule composition for treating the senile dementia, which is prepared from an active ingredient (-)-epigallocatechin gallate and pharmaceutically combinative auxiliary materials, and a method for preparing the soft capsule composition. The invention has an outstanding characteristic of providing an oral soft capsule with the advantages of safety, effectiveness, controllable quality and convenient use for senile dementia patients.
US8518887 Method of treating cancer with DLL4 antagonist and chemotherapeutic agent The invention provides methods for treating various types of cancer/tumor by administering the combination of Dll4 antagonists, in particular, Dll4 antibodies and fragments thereof that specifically bind human Dll4, and chemotherapeutic agents. Such combination therapies exhibit synergistic effects compared to the treatment with either agent alone. Thus, the methods of the invention are particularly beneficial for cancer patients who have low tolerance to the side effects caused by high dosages required for the treatment by either agent alone, by being able to reduce effective dosages. Pharmaceutical compositions and kits containing Dll4 antagonists and chemotherapeutic agents are also provided.
CN103446062A Preparing method of compound metformin hydrochloride and pioglitazone hydrochloride slow-release micro-pellet preparation The invention discloses a preparing method of a compound metformin hydrochloride and pioglitazone hydrochloride slow-release micro-pellet preparation. A metformin hydrochloride slow-release micro-pellet is prepared from two parts of a medicated pellet core and a slow release layer, wherein the medicated pellet core is prepared from metformin hydrochloride, a filler and a binder; the slow release layer is prepared from a sustained-release material and a pore-forming agent. A pioglitazone hydrochloride slow-release micro-pellet is prepared from three parts of a blank-pellet core, a medicated layer and a slow release layer, wherein the medicated layer is prepared from pioglitazone hydrochloride, a binder and a solubilizer; the slow release layer is prepared from a sustained-release material and a pore-forming agent. The effects of lasting drug release and a stable drug release behavior can be achieved in a human body; the bioavailability is relatively improved by the stable drug release behavior; the preparation is better in curative effect, small in toxic and side effects of drugs and better in hypoglycemic effect by compound combination of the two micro-pellets. The compliance of a sufferer is improved by delivery one time in a day; better dosage regimen and curative effect are provided for diabetes patients at home and abroad.
EP2531485A2 Highly selective 5-ht(2c) receptor agonists having antagonist activity at the 5-ht(2b) receptor Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.
WO2006082046A1 Use of s-clenbuterol The use of S-Clenbuterol for restoring and/or maintaining the function of partially or completely damaged/degenerated cells in the central nervous system and/or other nerve cells is claimed. The use of S-Clenbuterol leads to activation of astrocytes and initiation of endogenous processes of neuroprotection, it thus being possible for the damage or destruction of nerve cells to be reduced and, in some cases, even prevented.
WO2007048846A1 Use of iron-chelating compounds, cyclic adenosine monophosphate-increasing compounds or combinations thereof for treating axonal lesions in the cns The invention relates to cell implants and/or at least one pharmaceutically acceptable compound selected from the group consisting of iron chelating agents, cyclic adenosine monophosphate level-increasing compounds (CASEV), axon growth promoting compounds, inhibitors of the intracellular Rho signal path or combinations thereof for producing a drug for protecting neurons in the CNS that are damaged by axonal lesion from being destructed.
CA2170644C Multiple unit pharmaceutical preparation containing proton pump inhibitor A new pharmaceutical multiple unit tableted dosage form containing as active substance an acid labile H+K+-ATPase inhibitor or an alkaline salt thereof or one of its single enantiomers or an alkaline salt thereof, a method for the manufacture of such a formulation, and the use of such a formulation in medicine.
WO2008140052A1 Prophylactic or therapeutic agent for posterior ocular disease comprising ropinirole or salt thereof as active ingredient Disclosed is a novel prophylactic or therapeutic agent for a posterior ocular disease. Ropinirole or a salt thereof has an excellent anti-angiogenic activity and an excellent inhibitory effect on elevated vascular permeability in a posterior ocular tissue such as a choroid or a retina, and is therefore useful as a prophylactic or therapeutic agent for a posterior ocular disease such as age-related macular degeneration, diabetic retinopathy and diabetic macular edema.
WO2009010492A2 Combinations comprising telmisartan and an anticholinergic such as tiotropium or a glycopyrronium salt for the treatment of respiratory diseases such as copd or asthma The present invention relates to novel pharmaceutical compositions based on telmisartan 1 and anticholinergics 2 processes for preparing them and their use for the treatment of respiratory diseases.
US20120148521 Methods and Compositions for Controlled Release of Drugs Methods and compositions for controlled release of amine, alcohol and thiol drugs, e.g., narcotic analgesics, and tricyclic amine antidepressants, are provided. The drug is releasably covalently bonded to a polymer or other activity-blocking moiety. Release is by an unmasking reaction resulting in the formation of a chemical group that undergoes a second reaction releasing the drug. For example, the narcotic analgesic fentanyl covalently attached to an inert polymer by way of its nitrogen through formation of a quaternary vinylammonium salt is released by hydrolysis of an acetal exposing an alcohol that undergoes an intramolecular nucleophilic substitution reaction involving displacement of the fentanyl nitrogen. Process rate is controlled by controlling the rate of the intramolecular substitution reaction through varying the number of atoms in the chain connecting the alcohol group and the vinylic carbon and/or by the addition of substituents on that chain, and/or by the acetal hydrolysis rate.
US20090156665 Compositions Comprising Flavonoids and Toctrienols and Methods Thereof Disclosed in certain embodiments is a pharmaceutical formulation comprising a pharmaceutical ingredient comprising an active agent combination comprising flavonoids and tocotrienols in a ratio of about 75:25 to about 95:5 and at least one pharmaceutically acceptable excipient.
EP1716856A2 The treatment of acne A method of treating acne in a human in need thereof comprising administering systemically to said human a tetra-cycline compound in an amount that is effective to treat acne but has substantially no antibiotic activity, without administering a bisphoshonate.
CN101836969B Dry ice defatting pill The invention relates to a dry ice defatting pill as a defatting drug which is made by using dry ice as raw materials under a low temperature condition and is stored in a liquid nitrogen tank. The defatting pill comprises a casing, a sphere bag, a sphere bladder and dry ice. The dry pill defatting pill has an action principle of ensuring that the sphere bag is expanded in the stomach by the gasification of the dry ice, the expanded sphere bag floats on the upper part of food in the stomach and occupies partial space in the stomach to reduce the food intake of people, thereby achieving the purpose of defatting. When in use, the defatting pill is taken out of the liquid nitrogen tank, and patients rapidly take the defatting pill by using cold water when the surface temperature of the defatting pill reaches an above freezing temperature.
US20090088371 Combination therapy with syk kinase inhibitor The invention encompasses methods of increasing platelet levels in a patient having or at risk for immune thrombocytopenia comprising co-administering a Syk kinase inhibitor and a thrombopoietin receptor agonist, and methods of treating thrombocytopenia comprising co-administering a Syk kinase inhibitor and a thrombopoietin receptor agonist to a patient in need thereof, as well as pharmaceutical compositions for use in these methods.
WO2013090986A1 Treatment of seborrhoea A method for the treatment of seborrhoea in a patient comprises administering to the patient an effective amount of (24RS) or (24S) scymnol, an ester thereof or a pharmaceutically acceptable salt of a said ester, or of (24R) scymnol.
WO2008049073A2 Compositions for the treatment of inflammation in the brain and other tissues Methods of treating a patient who is predisposed to Alzheimer's Disease (AD) are disclosed. The methods include providing a patient determined to be predisposed t AD; and administering to the patient a therapeutically effective amount of an anti¬ inflammatory agent. The agent is preferably a TNFα inhibitor administered via a recombinant adenoviral-associated viral (rAAV) vector, by an intraparenchymal injection.
CA2073855C Glycoalkaloids for controlling cellular autophagy The invention is directed to the control of cellular autophagy, cellular agglutination and the immobilization of motile cells.Such control is useful in, for example, the treatment of cancer, contraception, termination of pregnancy, removal of pathogenic organisms and removal of any abnormal cellular growth (malignant or otherwise); as a diagnostic and analytical tool whereby cell structure can be studied and testing could be undertaken for the presence (and subsequent analysis) of pathogenic and non-pathogenic organisms; and in the manufacture of biochemicals whereby certain cells must be destroyed or otherwise contained.From surface analysis of normal and abnormal cells, specific receptors on abnormal cells which are either not present on normal cells or are only present insignificantly reduced numbers can be identified. Alkaloids and other pharmaceutically acceptable compounds are preferentially recognised by the abnormal cells, and which bind thereto and subsequently destroy.
US20110092567 Cannabinoid 2 (Cb2) Receptor Gene Promoter and Unique RNA Transcripts in B Cells and Methods of Use Cannabinoid receptor 2 (CB2) is expressed in B lymphocytes and is involved in immune regulation. Mouse splenic B cells express three CB2 transcripts utilizing two different first exons. Human peripheral blood B cells express one CB2 transcript utilizing one first exon. Alignment of sequenced RACE products to either the mouse or human genome reveals that isolated transcripts contain previously unidentified transcriptional start sites (TSS). B cells from mouse and human preferentially express one transcript, exon 1a in mouse and exon 1 in human. Multiple CB2 TSSs are utilized in mouse splenic B cells and one TSS in human peripheral blood B cells. The defining of the receptor gene TSSs in these cells provides materials and methods for therapeutically regulating immune function, including antibody isotype switching, using compounds such as inhibitory nucleic acids that down-regulate expression of the B cell CB2 gene (e.g., RNAi molecules).
CN101244170B Medicament for treating children's exogenous cough and preparation method The invention relates to a drug or a drug composition for treating exogenous cough, in particular to pediatric exogenous cough, as well as the preparation method. The drug is made of the active pharmaceutical ingredients according to the following parts by weight: 5 to 15 portions of herba schizonepetae, 10 to 20 portions of Japanese ardisia herb, 5 to 15 portions of ephedra (honey roast), 1 to 10 portions of bitter almond, 1 to 10 portions of baical skullcap root, 5 to 15 portions of nodakenin, 5 to 15 portions of French pinellia, 5 to 15 portions of pumise, 1 to 10 portions of cicada slough, 1 to 10 portions of tangerine or orange peel, 1 to 10 portions of alkanet and 1 to 10 portions of liquorice root.
US7897610 Use of benzo[c]quinolizinium derivatives for the treatment of diseases that are linked to smooth muscle cell constriction The invention relates to the use of benzo[c]quinolizinium derivatives for treating diseases that are linked to smooth muscle cell constriction, such as hypertension and asthma.
WO2007049121A1 Crystal form of sodium; (3r,5r)-7-[4-benzylcarbamoyl-2-(4-fluorophenyl)-5-isopropyl-imidazol-1-yl]-3,5-dihydroxy-heptanoate A crystal form A of sodium; (3R, 5R)-7-[4-benzylcarbamoyl-2-(4-fluoropheynl)-5-isopropyl- imidazol-1-yl]-3,5-dihydroxy-heptanoate is provided.
US7217729 4,6-Dimethyl-3-{[3'-(N,N-dimethylaminomethyl)-4-hydroxy-4'-(3''-methoxyphenyl)-cyclohexylamino]-methyl}-1H-indole 2-carboxylic acid ethyl ester or other derivatives of substituted indoles; for treatment or prevention of neurodegenerative diseases, psychological disorders, AIDS, inflammation or allergies Substituted indoles of the formula I, a process for the production of such compounds, pharmaceutical preparations containing these compounds and the use of these compounds for alleviating pain.
WO2011021224A3 Improved process for preparing (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[4-[2-(tetrazol-5-yl)phenyl]phenyl]methylimidazole-5-carboxylate Disclosed is an improved process for preparing (5-methyl-2-oxo-l,3-dioxolen-4-yl)methyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[4-[2-(tetrazol-5-yl)phenyl]phenyl]methylimidazole-5-carboxylate (formula-1, commonly known as "olmesartan medoxomil") through crystalline (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl 4-(1-hydroxy-1 -methylethyl)-2-propyl-1 -[4-[2-(trityltetrazol-5-yl)phenyl]phenyl]methylimidazole-5-carboxylate (commonly known as "trityl olmesartan medoxomil").
CN101343331B Synthesis of substituted pachyman The invention relates to a preparation method of polysaccharide, which aims at providing a synthetic method replacing pachymaran. In order to realize the purpose, the preparation method adopts the detailed technical steps: firstly, the ethanol aqueous solution of NaOH or NaOH/ urea aqueous solution is added in poria powder and is alkalified under the effect of ultrasonic wave for 30 minutes to 90minutes; secondly, the reaction reagent is added in a reaction system to react for 50 minutes to 90 minuets under the effect of ultrasonic wave and the temperature of 50 DEG C to 70 DEG C, the mol ratio of the NaOH and the reaction reagent is 2 to 6 : 1, and the use amount of the ethanol aqueous solution or the urea aqueous solution is 20 mL/1g to 30 mL/1g of poria powder; and thirdly, the targetproduct is obtained through leaching and acid washing the mixture obtained after reaction to neutrality and edulcoration. The preparation method has the advantages that the preparation method can perform one-step synthesis replacing pachymaran, the operation is convenient and time saving, and the cost is reduced; the ultrasonic wave is used to assist, the reaction speed is accelerated, and the substitution degree of the product is enhanced; the solution is secure, nontoxic and tractable.
WO2013033268A2 Bivalent bromodomain ligands, and methods of using same Described herein are compounds capable of modulating one or more biomolecules substantially simultaneously, e.g., modulating two or more binding domains (e.g., bromodomains) on a protein or on different proteins.
US20050042256 Food mixture; dietetics The present invention pertains to nutritional compositions containing specific blends of dietary lipids adapted to specifically influence the level of intramyocellular lipids in muscle tissue towards either higher concentrations or lower concentrations.
CN101502526A Application of mulberry twig flavone and diphenyl ethylene extract in preventing or treating hyperuricemia symptoms and uarthritis The invention discloses the components of mulberry branch flavone and stilbenes extract and a novel application thereof. According to the results of animal experiments, the mulberry branch flavone and stilbenes extract has no obvious effect on inhibiting the uric acid in the normal blood of normal animals, but reducing the uric acid in the blood of hyperuricemia model animals, thereby ensuring good safety. By compounding the mulberry branch flavone and stilbenes extract with relevant auxiliary materials, medicaments or health-care food and the combination of the medicaments or the health-care food with the compound being the active component for curing and controlling hyperuricemia and uarthritis can be prepared on the basis of the conventional preparation method, and have stable curative effect, are safe and reliable.
US20100303916 Enhanced drug delivery with orientable particles Small airway deposition of orientable drug particles in the lung due to interception is increased through alignment of these particles with an externally applied force such as a magnetic field. Drug particles in one embodiment are made magnetically responsive by loading them with magnetic nanoparticles. Elongated particles have a natural tendency to align parallel to the direction of flow through an airway, and therefore also parallel to airway walls; accordingly, alignment with a magnetic field to any other orientation increases interception, with a maximum increase for alignment perpendicular to airway walls. By positioning a magnetic field across a specific site within the lung, for example in the area of a tumor, the increase in deposition by interception allows localized targeting of inhaled drug particles to that area.
US20120196921 Modulation of sglt-2 expression Compounds, compositions and methods are provided for modulating the expression of SGLT2. The compositions comprise oligonucleotides, targeted to nucleic acid encoding SGLT2. Methods of using these compounds for modulation of SGLT2 expression and for diagnosis and treatment of diseases and conditions associated with expression of SGLT2 are provided.
WO2014100314A1 Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Cy, and the subscript t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
US20080317673 Method for diagnosing and treating bronchial asthma A method for diagnosing and treating a bronchial asthma by classifying a patient's asthma as Type I, Type II or Type III based on the patient's symptoms is disclosed. The symptoms for the three types of asthma are disclosed together with recommended treatment guidelines for each type to optimize treatment regiments based on symptoms.
CN103690927A Application of bortezomib in preparation of medicaments for preventing or treating giant cell tumor of bone The invention belongs to the technical field of medicines. The invention provides an application of bortezomib in preparation of medicaments for preventing or treating giant cell tumor of bone (GCTB). According to the application provided by the invention, the treatment effect of the bortezomib against the GCTB is researched from two aspects of in-vitro cell culture and in-vivo animal experiments, the possible action mechanism is investigated from the molecular level, and the experimental results show that the bortezomib can be used for inhibiting the formation of osteoclasts of the GCTB and the absorption of osteocomma, inducing stromal cell apoptosis and inhibiting the proliferation of stromal cells.
WO2008001929A1 Treatment agent for inflammatory bowel disease A treatment agent for inflammatory bowel disease containing, as an active ingredient, a p38 MAP kinase inhibitor having a property as an antedrug is disclosed.
WO2008045135A2 Systems providing antimicrobial activity to an environment A process reduces the microbial content in land mass by providing molecular iodine in the land mass in a concentration in aqueous material in the land mass of at least 10 parts per million. The molecular iodine may be added in gaseous or liquid or solid state, and may be formed in situ in the land mass using available water in the reaction.
US20120095002 Isoxazole-5-carboxamide derivatives The present invention relates to isoxazole-5-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-5-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.
CN101780064A New application of p-hydroxyl cinnamic acid The invention discloses a new application of p-hydroxyl cinnamic acid in preparing a medicament for preventing and curing viral diseases or bacterial diseases of livestock and poultries. The product can prevent and cure viral and bacterial diseases of the livestock and the poultries and improve the production performance of the livestock and the poultries. Proved by in vivo and in vitro experiments, the p-hydroxyl cinnamic acid has the effects of preventing and curing diseases caused by mycoplasma gallisepticums, cow escherichia coli, and the like. Proved by in vivo experiments, the p-hydroxyl cinnamic acid has the effects of preventing and curing Fabricius bursal viral diseases of the livestock and the poultries, avian mycoplasmosis and avian influenza H9 and H5 subtype virus infections.
US20110275719 Novel trifluoromethylsulfonamide gamma secretase inhibitor The present invention is directed to a novel trifluoromethylsulfonamide derivative which inhibits the processing of APP by the putative γ-secretase and thus is useful in the treatment or prevention of Alzheimer's disease. This compound possesses favorable pharmacokinetic properties in higher species (rhesus) and thus can be dosed on an intermittent dosing regiment (e.g., once weekly). When dosed on such a regiment the compound exhibits significant and continuous Aβ lowering without the manifestation of Notch associated gastrointestinal toxicity for extended periods, e.g., 7 days. Pharmaceutical compositions and methods of use are also included.
CN101925573A Novel N-(2-amino-phenyl)-amide derivatives The present invention provides novel compounds of the general formula (I), and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments, containing them. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.
CN101919845A Application of matrine compound in preparing anti-prostate tumor drug The invention discloses an application of a matrine compound in preparing an anti-prostate tumor drug. The matrine compound is matrine or oxymatrine which is obtained through screening, can explicitly inhibit prostate specific antigens, and has exact curative effect on human body prostate tumor. Compared with the existing botanical drugs for treating the prostate tumor, the matrine compound of the invention has more clear mechanism of action and exact curative effect, and has the potential of further modifying molecular structure and improving drug effect, thus the matrine compound can be applied to preparing the anti-prostate tumor drug.
US7776867 Furanopyrimidines The present invention relates to furanopyrimidine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula I. The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula I.
CN102516333A Diphyllin1,2-trans-permethoxy glucoside, its preparation method and application thereof The invention discloses diphyllin1,2-trans-permethoxy glucoside, its preparation method and an application thereof. The structural formula of diphyllin1,2-trans-permethoxy glucoside is as shown in the formula (1), in which R is tetramethoxy-beta-D-glucosyl, tetramethoxy-beta-D-galactosyl, tetramethoxy-alpha-D-mannosyl, trimethoxy-beta-D-quinoloneglycosyl, heptamethphoxy-beta-D-galactose, trimethoxy-alpha-L-Aralino, trimethoxy-alpha-L-rhamnosyl or trimethoxy-beta-L-fucosyl. Diphyllin1,2-trans-permethoxy glucoside is convenient to prepare and has an effect of inhibiting growth of tumor cells.
US7304077 Asthma, rhinitis therapy The invention provides compounds of formula (I): as modulators of chemokine and H1 receptor activity. The compounds are especially useful in the treatment of asthma and rhinitis.
CN101396540B Medicine composition for treating hyperplasia of mammary glands and preparation method thereof The invention discloses a pharmaceutical composition for treating breast hyperplasia, and the pharmaceutical composition is composed of raw rehmannia root, costustoot, figwort root, blister beetle, forsythia, rhubarb, Japanese ampelopsis root, tangerine peel, green tangerine peel, raw liquoric root, unibract fritillary bulb and other medicines. The pharmaceutical composition has the effect on activating blood circulation, removing blood stasis, activating qi and relieving pain for treating the breast hyperplasia and can expand the capillary vessels, accelerate the blood flow velocity and improve the microcirculation; the pharmaceutical composition can rapidly get through the obstructed glandular tubes and gradually soften the masses till the disappearance, patients can be recovered completely and the relapse is difficult after the healing.
CN102247340A Application of apogossypol ketone in preparation of drugs for treating tumor diseases The invention relates to an application of apogossypol ketone, and specially relates to an application of apogossypolic ketone in preparation of drugs for treating tumor diseases. Apogossypol ketone can effect on Bcl-2, Mcl-1, Bcl-XL or Bcl-w, and prevent them to combine with a pro-death protein BH3-only so that the pro-death protein is released to participate in an apoptotic response. Whether apogossypol ketone is utilized for drugs alone or in combination, apogossypol ketone can show an antineoplastic activity for an animal tumor model.
EP1088084B1 Erythropoietin analog-human serum albumin fusion protein Erythropoietin analog-human serum albumin (EPOa-hSA) fusion protein and methods of making and using the fusion protein.
WO2008004231A1 Anti-cancer therapy comprising an h2-blocker, at least one antiinflammatory agent and a cytotoxic agent The present invention relates to the treatment of a mammal with a pharmaceutical composition comprising an H2-blocker, at least one anti-inflammatory agent, a cytotoxic agent and, optionally, levamisole, a retinoid, an NFkB inhibitor, a redox quinone, an agent that enhances the intracellular accumulation of NADH + H+, a poly-alcohol, an inhibitor of pro-angiogenic growth factor(s) and an MMP inhibitor, such pharmaceutical composition allowing for the enhanced therapy and/or prevention of neoplastic diseases and disorders.
CN103028016A Preparation technology and production method of integrated new dosage form of Pinellia Tuber and sulfur pill The invention relates to a preparation technology and a production method of an integrated new dosage form of a Pinellia Tuber and sulfur pill. The raw materials for the effective components of the pill comprise 10 parts by weight of (ginger processed) Pinellia Tuber and 10 parts by weight of (processed) sulfur. The production method comprises the production processes of ultrasonic airflow crushing, alcohol-water extraction, supersonic wave crushing extraction, water decoction and concentration, ultrasonic spray drying, nanometer grinding, high-pressure homogenization, nanoparticle preparation and the like. The advantages comprising multiple cooperation, multiple targeting and the like of a nanometer carrier combination technology are utilized in the invention. Great production cost reduction, great product quality improvement, medicine targeting strengthening, and medicine sustained and controlled release property strengthening are realized after the large-scale production. Internal and external administration can be simultaneously carried out, and the pill can be respectively administrated in four time periods according to the midnight-noon ebb-flow and human qi and blood flow rules. The pill can also be processed to prepare a film agent and a transdermal agent which are respectively plastered on different positions of a human body according to the midnight-noon ebb-flow and human qi and blood flow rules, and the effective components can be directly absorbed through skins.
CA2282439C Formulations for hydrophobic pharmaceutical agents The field of the invention is inducible gene expression systems wherein expression is controlled by a novel ecdysone receptor or its derivatives. The field particularly relates to the isolation and characterization of nucleic acid and polypeptides for a novel ecdysone receptor. The nucleic acid and polypeptides are useful in novel gene expression systems inducible with ecdysone or derivative receptor agonists.
EP2760856A1 Selective nr2b antagonists The disclosure generally relates to compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
WO2011021218A3 Process for preparing 4-[3, 5-bis (2-hydroxyphenyl)-lh-l, 2, 4- triazol-i-yl] benzoic acid and its amine salts An improved process for preparing 4-[3, 5-bis (2-hydroxyphenyl)-l, 2, 4-tπazol-l -yl] benzoic acid of formula-1 and a process for its purification are provided The preparation process comprises reacting salicylic acid with salicylamide in the presence of a suitable base, in a suitable solvent and in the presence of thionyl chloride at reflux temperature, then reacting 2-(2-hydroxyphenyl)-benz[e][l,3]oxazin^-one with 4-hydrazinobenzoic acid in a suitable alcoholic solvent at reflux temperature to provide deferasirox.
WO2014069837A1 Histamine receptor antagonist composition containing gamma oryzanol as active ingredient The present invention provides a novel use of gamma oryzanol as a histamine receptor antagonist. Gamma oryzanol is used as a natural antihistamine and can be used for preventing or treating allergic rhinitis, inflammatory bowel diseases, asthma, bronchitis, vomiting, stomach and duodenal ulcer, gastoesophegal reflux diseases, sleep disturbance, anxiety, and depression, and has the advantages of further reducing sleep latency, increasing sleep time, and increasing non-REM sleep time. Gamma oryzanol is a natural product derived from rice bran and does not cause side effects such as cognitive impairment, resistance, or dependence even after long-term use.
CN101385706A Anticancer composition loaded with melphalan and fotemustine An anticancer composition carrying melphalan and fotemustine is a sustained release injection which consists of sustained release microspheres and a dissolvent, wherein, the sustained release microspheres comprise an anticancer active component and a sustained release adjuvant, and the dissolvent is a common dissolvent or a special dissolvent containing a suspending agent. The suspending agent has the viscosity of 100cp-3000cp (at the temperature of 20-30 DEG C) and is selected from sodium carboxymethyl cellulose and the like; the anticancer active component is a combination of a nitrosourea drug and an alkylating agent selected from the melphalan, ifosfamide, 4H-peroxy-cyclophosphamide or norcantharidin; the sustained release adjuvant is selected from copolymer of such polyphosphate esters as p(LAEG-EOP), p(DAPG-EOP) and the like, or copolymer of the polyphosphate esters and polylactic acid, polifeprosan, dienoic fatty acid and sebacic acid, or copolymer or polyblend of poly(erucic acid dimmer-sebacic acid) or poly(fumaric acid-sebacic acid); the anticancer composite is also made into a sustained release implant, and injected into or placed inside or at the periphery of tumor to keep the effective drug concentration more than 60 days, The anticancer composite can also obviously reduce the general reaction of the drug, and selectively enhance the curative effects of non-operative therapies such as radiotherapy, chemotherapy and the like.
CN101182289B 4'-hydroxy-4,6'-dimethoxy dihydrocharcone and method for synthesizing the same The present invention discloses a 4'-hydroxy-4, 6'-dimethoxy dihydrochalcone and a synthesis method thereof. The present invention considers 4-benzyloxy-2-hydroxy hypnone as the raw material to be processed for the methylation reaction when the two phases of lye and organic solvent exist, and 4-benzyloxy-2-methoxy hypnoone is obtained. Then the 4-benzyloxy-2-methoxy hypnoone and 4-methoxy benzaldehyde are processed for the aldol condensation reaction in alkaline alcohol solution to obtain a intermediate product of 4'-benzyloxy-4, 6'-dimethoxy chalcone, then the intermediate is hydrogenated tobe deoxidized when catalyst Pd/C exists, and protective group is removed from the intermediate, and finally a target product of the present invention of the 4'-hydroxy-4, 6'-dimethoxy dihydrochalconeis obtained. The operation of the method of the present invention is safe, simple and convenient; the obtained product has the high purity, the good safety of animal acute toxicity test and the good activity of resisting the platelet aggregation.
WO2014154683A1 Pharmaceutical formulation comprising phosphatidylcholine for the treatment of ulcerative colitis A pharmaceutical formulation, comprising a phosphatidylcholine product of formula (I), wherein R1 is the residue of a saturated or unsaturated fatty acid with 12-24 carbon atoms, and R2 is the residue of a saturated or unsaturated fatty acid with 12-24 carbon atoms, and wherein the phosphatidylcholine product (PC) contains the following amounts of fatty acids: 55 –72 linoleic acid; 10 –18 palmitic acid; 07 –15 oleic acid; 02 –08 linolenic acid; 02 –08 stearic acid, and at least one excipient for delayed release, can be used for the improved treatment of ulcerative colitis.
US8114892 Methods and compositions for the treatment of Parkinson's Disease The invention features methods and kits for treating or inhibiting the development of Parkinson's Disease by administering 7-chloro-4-aminoquinoline compounds, e.g., amodiaquine or glafenine. Stem cells are also useful in the methods of the invention and may be administered separately from or together with 7-chloro-4-aminoquinoline compounds. The invention further features methods of identifying additional chemical compounds that are useful in the treatment or inhibition of the development of Parkinson's Disease.
EP2513058A1 Methods of synthesizing factor xa inhibitors Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof.
CN100999496A Compound of polyphenols with aza-containing heterocyclic modified and use thereof This invention relates to a nitrogen-containing heterocyclic modified polyphenolic compounds and its applications. Its purpose is to provide a nitrogen-containing heterocyclic modified polyphenolic compounds and applications in the preparation of Alzheimer's disease, Parkinson's disease and other degenerative nervous system disease or type two diabetes preventing and treatment drug. Studies show that the polyphenolic compounds can inhibit aggregation of A beta, also can make the A beta aggregated depolymerize, and will eventually eliminate hydrolysis A beta protein, inhibited and removal of beta A toxicity, in the field of medicine has broad application prospects.
US20110237527 Sglt-2 inhibitors, methods of making them, and uses thereof The present invention relates to compounds which are inhibitors of sodium dependent glucose co-transporter-2 (SGLT-2). These compounds are used in the treatment of various disorders, including diabetes, impaired glucose tolerance, insulin resistance, retinopathy, nephropathy, neuropathy, cataracts, hyperglycemia, hyperinsulinemia, hyperchlolesterolemia, elevated blood level of free fatty acids or glycerol, hyperlipidemia, hypertriglyceridemia, obesity, wound healing, tissue ischemia, atherosclerosis, and hypertension. These compounds and compositions are also useful for treating and preventing kidney stones, hyperuricemia, gout, and hyponatremia. Methods of making these compounds are also described in the present invention.
CN103054901A Dialysates and methods and systems related thereto Compositions, systems, and methods of treating conditions such as vascular calcification conditions are disclosed. A representative method includes administering to an individual in need of treatment an effective amount of at least one effector agent. Another method includes prophylactically treating vascular calcification or vascular calcification-related conditions by administering to an individual in need of treatment an effective amount of at least one effector agent. Still another method includes treating vascular calcification by administering an effective amount of at least one effector agent to an individual in need of treatment via hemodialysis.
CN1590545A Small interference RNA molecule (siRNA) of attacking SARS virus mRNA melecule and application A small-interference ribonucleic acid (SiRNA) molecule able to attack the mRNA molecular of SARS virus and its application in preparing the medicines for treating SARS and its virus infection associated diseases are disclosed. Said SiRNA is a double-stranded RNA molecule.
WO2008132710A3 Pharmaceutical nimodipine compositions A modified release solid dosage product comprises a plurality of minicapsules or minispheres containing nimodipine, wherein when exposed to a use environment more than 40% of the nimopodine is released within 12 hours and wherein the Tmax is reached within 6 hours. The product may be a capsule 4 having a first population of uncoated minispheres 1 containing nimodipine for immediate release and a second population of coated minispheres 2 containing nimodipine for sustained release. There may be another population of coated minicapsules 3.
EP0863768B1 Covalent heparin-protein conjugates comprising an alpha-carbonyl amine bond and methods of obtaining them Novel conjugates of glycosaminoglycans, particularly heparin and dermatan sulfate, and amine containing species and therapeutic uses thereof are described. In particular, mild methods of conjugating heparins to proteins, such as antithrombin III and heparin cofactor II, which provide covalent conjugates which retain maximal biological activity are described. Uses of these conjugates to prevent thrombogenesis, in particular in lung airways, such as found in infant and adult respiratory distress syndrome and on surfaces in contact with blood are also described.
WO2008115999A8 Biaryl and biheteroaryl compounds useful in treating iron disorders This invention is directed to compounds of formula (I), wherein A, B, m, n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.
US20110257117 Olive compositions and methods for treating inflammatory conditions A method of treating an inflammatory condition with a hydroxytyrosol-rich composition. Improvement is monitored as a reduction in the levels of a biochemical marker such as homocysteine or C-reactive protein. The composition may be administered in an amount and for a period sufficient to effect a drop in the level of the biochemical marker.
US7736873 An isolated nucleic acid molecule comprising a nucleotide sequence which encodes the polypeptide comprising the outer membrane protein antigens of gramnegative bacteria, which can be used to prevent and treat gramnegative bacteria infection in mammals, such as humans; immunology; vaccines The present invention provides a method of nucleic acid, including DNA, immunization of a host, including humans, against disease caused by infection by a strain of Chlamydia, specifically C. pneumoniae, employing a vector containing a nucleotide sequence encoding a 98 kDa outer membrane protein of a strain of Chlamydia pneumoniae and a promoter to effect expression of the 98 kDa outer membrane protein gene in the host. Modifications are possible within the scope of this invention.
EP1474120B1 Antibody having a t-cell receptor-like specificity, yet higher affinity, and the use of same in the detection and treatment of cancer, viral infection and autoimmune disease An isolated molecule which comprises an antibody specifically bindable with a binding affinity below 20 nanomolar, preferably below 10 nanomolar, to a human major histocompatibility complex (MHC) class I being complexed with a HLA-restricted antigen and optionally further comprises an identifiable or therapeutic moiety conjugated to the antibody.
US7608683 Human leukocyte antigen pan DR-binding peptides for use in the treatment of infections, inflammatory, autoimmune and cancer diseases; has heat shock protein that is capable of binding to MHC class II molecules Provided are HLA pan DR-binding peptides and methods of using such peptides to modulate, block, or inhibit immune responses to effect treatment of immune-mediated diseases and conditions, such as inflammatory and autoimmune diseases, cancer, and microbial infections. These peptides and methods are also useful diagnostically to screen peptide or peptide analogs that can inhibit the pathogenic immune response or up-regulate an immune response against aberrant or invading cells, to monitor efficacy for therapeutic treatments, and to identify other agents that may be effective to inhibit or otherwise modulate an immune response such as by altering T cell functional phenotype, and even more particularly by modulating the regulatory phenotype of regulatory T cells and/or inducing emergence of T cells with a different functional phenotype.
US20070123491 Podophyllotoxin derivatives as igf-1r inhibitors The invention refers to new compounds, e.g. podophyllotoxin derivatives, as well as to the use thereof and of known compounds as specific inhibitors of the insulin-like growth factor-1 receptor (IGF-1R). Said compounds can be used for treatment of IGF-1/IGF-1R dependent diseases, such as cancer, psoriasis, arteriosclerosis, certain endocrine and metabolic disorders etc.
US7008633 Injection of a biocompatible polymer, polysaccharide or polyamino acid, a cross-linker, and therapeutic agent into tumor; hydrogel formed in the tumor retains the therapeutic agent Methods regarding local regional treatment in situ for an individual, such as of a tumor, are provided herein. A hydrogel composition is generated in situ in the tumor by administering a polymer, such as a polysaccharide or a polyamino acid, with a therapeutic agent, such as a radionuclide or a drug, and administering a cross-linking agent. The hydrogel/therapeutic agent composition is retained in the tumor for safe and efficient tumor therapy. Alternatively, a hydrogel composition is generated in situ in an artery which nourishes a tumor to occlude the artery.
CN102382076A Arone and arylamide compound and preparation method and medicine use thereof The invention discloses a novel arone and arylamide compound represented by formula I, a cistrans isomer, physiologically acceptable salts, a solvate and a crystallizing form thereof, a preparation method of the compound, a medicine preparation containing the compound and clinical application of the compound in treating diseases related to protein tyrosine phosphatases 1B.
WO2005123681A1 Saturated and unsaturated 3-pyridyl-benzocycloalkylmethyl-amines for use in the treatment of pains, depressions and anxiety states The invention relates to the saturated and unsaturated 3-pyridyl-benzocycloalkylmethyl-amines of general formula (I), to methods for producing drugs containing said compounds, to the use of saturated and unsaturated 3-pyridyl-benzocycloalkylmethyl-amines in the production of drugs and to methods for treating pains, depressions and/or anxiety states.
CN1621040A Antemetic Granisetron Hydrochloride tablet and its preparation The orally disintegrated granisetron tablet as antiemetic is prepared with granisetron hydrochloride as main medicine component, hydroxyethyl cellulose and other medicinal supplementary material. After being taken, the antiemetic may be disintegrated fast in orally and swallowed into digestive tract without need water to produce excellent effect of preventing and treating nausean and vomiting caused by chemotherapy, radiotherapy and surgical operation. The present invention has low production cost.
EP2308848A1 Quinoline-derived amide modulators of vanilloid VR1 receptor This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to quinoline-derived amides that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
CN103191105A Application of furocoumarin compounds in preparation of anti-hepatitis B virus (HBV) medicaments The invention relates to the field of medicament application, and in particular discloses application of furocoumarin compounds in preparation of anti-hepatitis B virus (HBV) medicaments. The compounds are different from current commercial anti-HBV medicaments, and belong to non-nucleoside compounds; cytological experimental studies show that the compounds can inhibit the replication of HBV DNA (deoxyribonucleic acid) and the secretion of HBsAg and HBeAg; and cytotoxicity tests show that the compounds have very low toxicity, so the compounds can be safely used for preparing the medicaments for treating and/or preventing related diseases caused by HBV infection.
US20060223779 Method of screening for inhibitors of human Fatty Acid-CoA Ligase 4 The present invention provides a method of screening for potential cancer chemotherapeutic and chemopreventive agents which act by modulating the activity of the Fatty Acid-CoA Ligase 4 (FACL4) gene product in humans. This invention also provides methods of administering such agents to treat cancer by inhibiting the activity of the FACL4 gene product, thus raising the cellular level of free arachidonic acid and triggering arachidonic acid-mediated apoptosis. The present invention further provides a method for diagnosing cancers, including colon cancer.
US20120095104 Use of vasoconstrictors There is disclosed the topical dermal use of vasocontrictor substances for regulating body temperature to treat, prevent or delay the onset of anesthetic induced hypothermia. Kits containing appropriate materials and instructions, and other embodiments, are also disclosed.
WO2006022173A1 HUMECTANT CONTAINING α-GLYCOSYL GLYCYRRHIZIN AS ACTIVE INGREDIENT AND USE THEREOF A humectant which is applicable to formulations for external-use skin preparations, has humectant activity, and gives no tacky feeling; and a skin preparation for external use which contains the humectant. The tack-free humectant contains α-glycosyl glycyrrhizin as an active ingredient. It is satisfactory in applicability and cosmetic finishing, imparts softness and tension to the skin, and has satisfactory humectant properties.
CN1830429A Medicinal chewing tablet used for antipyretic analgesic and its preparation method A medicine in the form of chewing tablet for antipyresis and anodyne is prepared from ibuprofen through including it in cyclodextrin, mixing with filler and flavouring, granulating and die pressing.
CN101594868A A pharmaceutical composition having antipsychotic, antidepressant or antiepiieptic activity with reduced side effect The side effect leading to overweight or obesity in medication with a known antipsychotic, antidepressant or antiepileptic drug is reduced by the administration of O-(3-piperidino-2-hydroxy-1-propyl)-nicotinic amidoxime or a pharmaceutically acceptable acid addition salt thereof.
EP0859777B1 8-azabicyclo(3.2.1)oct-2-ene derivatives, their preparation and use A compound having formula (I) or any of its enantiomers of any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; and R4 is phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF¿3?, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; or naphtyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter re-uptake inhibitors.
CN102908335A Rosuvastatain calcium composition and preparation method thereof The invention relates to the field of medicine, and in particular relates to a rosuvastatain calcium composition and a preparation method of the composition. The invention provides a rosuvastatain calcium composition which contains rosuvastatain calcium and calcium sulfate. When the rosuvastatain calcium composition is prepared, a NaOH solution is taken as a pH conditioning agent, so that the stability of the rosuvastatain calcium is guaranteed, and the pharmaceutical composition is more easily pelletized; and the CaSO4 has the protection function, so that the medicine stability is further improved. Furthermore, the conventional technology is adopted by the invention, the operation is simple, and large-scale production is very easily realized.
WO2009086055A1 Enhancing photostabilization of oxymetazoline The photostability of oxymetazoline in a topical decongestant composition is enhanced by lowering the pH of the composition using a buffer solution.
CN102793662A Probucol nano suspension and preparation method thereof The invention relates to hydrophobic medicine probucol nano suspension and a preparation method thereof. The probucol nano suspension is a semi-transparent opalescent solution consisting of 1 part of probucol, 0.1 to 1,000 parts of surfactant and 20 to 1000 parts of water. The probucol nano suspension is prepared by a self-assembly technology, and the prepared nano suspension is small in particle size. According to the probucol nano suspension, the particle size of an insoluble medicine probucol is reduced, the specific surface area of the medicine is increased, the medicine can be easily absorbed in a human body, and the bioavailability of the medicine can be improved. Compared with probucol suspension, the probucol nano suspension has the advantages that the bioavailability of the probucol nano suspension in bodies of mice can be improved by 3 to 14 times, and the curative effect of the probucol nano suspension can be fully exerted.
EP2121658A2 Piperazinyl-propyl-pyrazole derivatives as dopamine d4 receptor antagonists, and pharmaceutical compositions containing the same The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.
WO2014106848A1 Coumestan, coumestrol, coumestan derivatives and processes of making the same and uses of same The present invention provides new coumestans compounds and processes for the preparation of coumestans, pharmaceutical compositions having a coumestan as an active pharmaceutical ingredient, and methods of utilizing coumestans as selective estrogen receptor modulators (SERMs) for treating estrogen dependent diseases such as breast cancer.
US7585869 novel bicyclic derivatives that are useful in the treatment of abnormal cell growth, such as cancer; tyrosine kinase inhibitors The invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R11, N, Z, A, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
CN1785191A Zalaipulong injection A Zhalaipulong injection for the inducing of general anesthesia and treating epilepsy, convulsion, and minimal convulsion caused by tetanus contains proportionally the Zhalaipulong as active component and the solvent chosen from water-soluble or water-insoluble solvent and the water for injection.
CN103381189A Porous hemostatic powder and its preparation method The invention provides a porous hemostatic powder which is prepared by carrying out physical drilling on a soluble material to form porous microspheres. A preparation method of the porous styptic powder comprises the following steps: putting the soluble material on a supersonic vibration bed device, starting the device, vibrating, and simultaneously carrying out laser radiation for 10-60 min. The soluble material undergoes laser drilling. The preparation method has advantages of simple technology, easy operation, low production cost and wide raw material sources. Soluble starch, carboxy methyl starch, hydroxyethyl starch, carboxymethylcellulose sodium, ethyl cellulose or sodium alginate and their derivatives are medically proved to be safe medical materials, are generally used as pharmaceutic adjuvants and sustained release agents of medicines, and are also used to prepare absorbable hemostatic gauze such as Tailing absorbable hemostatic gauze. These materials are all dissoluble; the size of molecular weight is controllable; preferably, the molecular weight is 500-12000Dalton; more preferably, the molecular weight is 1000-40000 Dalton; and the materials all can be absorbed by body.
WO2009097682A8 Anti-influenza compounds The present invention provides pyrimidinyl compounds of formula (I) and pharmaceutically acceptable salts thereof. These compounds may be used for the inhibition of influenza. In particular, the compounds of the invention may be used for the treatment or prophylaxis of influenza A, most particularly H1N1 or H5N1 influenza. The compounds of the invention can also be used for the treatment or prophylaxis of a disease caused by Vibrio cholerae, Clostridium perfringens, Streptococcus pneumoniae, Arthrobacter sialophilus, an orthomyxovirus, a paramyxovirus, a parainfluenza virus, mumps virus, Newcastle disease virus, fowl plague virus or Sendai virus.
US20080031955 Product Comprising a Beta-Lactam Antibiotic The present invention relates to a product comprising a β-lactam antibiotic, for instance a cephalosporin, said product containing less than 200 mg of acetone per kg of β-lactam antibiotic. The invention also relates to a process for drying a β-lactam antibiotic, for instance a cephalosporin, said process comprising drying said β-lactam antibiotic under decreased pressure.
US20080200421 Heparin linked to bioabsorbable polylactone; restenosis prevention; stent implants; synthesis A conjugate between an anti-thrombotic agent and a bioabsorbable polymer is provided. In addition, a method is provided for applying a coating comprising an anti-thrombotic agent and a bioabsorbable polymer conjugate to at least a portion of an implantable device to prevent or reduce the formation of thrombosis on the surface of the device. A first or sub-layer of the coating is prepared by mixing a polymeric material and a biologically active agent with a solvent, thereby forming a homogeneous solution. A second or outer layer comprises an anti-thrombotic heparin-bioabsorbable polymer conjugate. This coating may be applied over the inner drug-containing layers using, for example, a dip coating or spray coating process. After drying, the anti-thrombotic heparin bioabsorbable polymer conjugate remains in the outer layer of the coating, allowing agent from the inner layer to be eluted there through. In addition, the outmost layer prevents the formation of thrombosis, and also serves to modulate the release kinetics of the agent(s) contained within an inner layer(s) of the coating.
US6906058 Prevent bile acid transportation; anticholesterol agents The present invention relates to compounds of formula (I) wherein R1 and R2 are independently selected from C1-6alkyl; one of R4 and R5 is a group of formula (IA): R3, R6, R7, R8, R9, R10 and R11 and the other of R4 and R5 are as defined within, pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and there use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.
CN103159721A 8-epi-12-epi-isoandrographolidume-19-sulfate, preparation method and purposes of prepared medicine The invention discloses 8-epi-12-epi-isoandrographolidume-19-sulfate or salt thereof, a preparation method thereof, and antipyretic, anti-inflammatory and antiviral purposes of the 8-epi-12-epi-isoandrographolidume-19-sulfate or the salt thereof. The 8-epi-12-epi-isoandrographolidume-19-sulfate or the salt thereof formed by the preparation method does not change chemical properties of andrographolidume, the 8-epi-12-epi-isoandrographolidume-19-sulfate or the salt thereof has the advantages of being good in water-solubility, high in heat stability, small in hemoclasis, and the like, and pharmacoactive effects of andrographolidume pure natural medicine are guaranteed to the greatest extent. In addition, medicine and pharmaceutical research workers cannot know the good purposes of 8-epi-12-epi-isoandrographolidume-19-sodium disulfate in advance on the premise that related experiments are not conducted.
US8247407 Pharmaceutical composition with anti-diabetic action The invention relates to medicine, in particular to searching and developing novel medicinal agent for treating pancreatic diabetes. The invention is based on the development of more effective and less toxic medicinal agents based on indole derivatives which exhibit antidiabetic, hypolipidemic, hypoglycemic, hypocholesterolemic activity and insulin resistance-improving actions and the structure of which differs from the structure of traditionally used compounds. The inventive indole derivatives are also low-toxic and easily tolerated.
US20100179165 Methods for treating inflammatory disorders using 2,4-pyrimidinediamine compounds Methods for treating an inflammatory disorder and for inhibiting the production of IL-23 using 2,4-pyrimidinediamine compounds represented by formula (I):
CN102342914A Calcipotriol solid lipid nanoparticle and preparation method of same The invention relates to a calcipotriol solid lipid nanoparticle and a preparation method of the same. The calcipotriol solid lipid nanoparticle consists of the following components in percentage by weight: 0.005-0.5% of calcipotriol, 0.1-30% of lipid material, 0.5-10% of surfactant and water. The calcipotriol solid lipid nanoparticle provided by the invention is prepared by a high-pressure homogenization method or a microemulsion method, is easy to realize industrial production, and can be further used for preparing external emulsifiable paste or gels for the treatment of psoriasis and ichthyosis. The calcipotriol solid lipid nanoparticle has the advantages that: the calcipotriol is wrapped in the solid lipid nanoparticle, and can be used for carrying medicines to penetrate through a horny layer so as to improve the skin keratin penetrating capacity of the medicines, so that the medicines can be retained at a local part of skin (cuticular layer and derma) for a long time, and the concentration of therapeutic medicines at the local part of the skin is improved; and therefore the therapeutic effect of the medicines is increased, and action time of the medicines is extended.
WO2010008832A1 Pyrrolo-pyridine-3-yl-piperazine derivatives having 5-ht6 receptor affinity The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I); wherein R1, R2, Ar, m and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
WO2013191565A1 Antimicrobial composition and its method of use This invention relates to an anti-microbial composition including at least a) melaleuca oil, or an isolated fraction or an active agent or equivalent thereof; b) manuka oil, or an isolated fraction or an active agent or equivalent thereof; and c) at least one galloyl moiety.
CN101607960B Acebrophylline and composition thereof The invention relates to a crystal form of acebrophylline, surfolase and a preparation method thereof. The invention also relates to a pharmaceutical composition containing the crystal form and the application of the new crystal form in the preparation of medicine which is used for relieving cough and eliminating phlegm as well as has double functions of bronchiectasis and mucolysis.
CN103006674A Compound sulfamonomethoxine sodium solution and preparation method thereof The invention aims to disclose a compound sulfamonomethoxine sodium solution and a preparation method of the compound sulfamonomethoxine sodium solution. The compound sulfamonomethoxine sodium solution comprises 100ml of the following components: 5-20g of sulfamonomethoxine sodium, 1-5g of trimethoprim, 20-70ml of an organic solvent, 0.1-0.5g of an antioxidant and 0.1-0.5g of a metal complex. Compared with an injection liquid, the prepared compound sulfamonomethoxine sodium solution has the advantages of convenience for administration, resource economization, wide application, strong product activity, high bioavailability, stable efficacy, obvious effect, stable shape and properties, slow degradation of main drugs, capability of continuously keeping bioactivity and the like, and thus the aim of the invention is realized.
CN102600188A Novel application of stilbeneglycoside to antidepressant medicament The invention provides a novel application of stilbeneglycoside to an antidepressant medicament. The stilbeneglycoside has low toxicity, and does not have the defects of calming, ataxia, induction of epilepsy and the like existing in the conventional antidepressant medicament. The stilbeneglycoside can be applied to preparation of a medicament for preventing and/or treating depression. The stilbeneglycoside can be added into a pharmaceutically-acceptable salt, ester or sugar for preparing a medicament for preventing or treating an antidepressant state. The stilbeneglycoside and the pharmaceutically-acceptable salt, ester or sugar thereof can be prepared into pharmaceutically-acceptable dosage forms such as tablets, capsules, oral liquids, injections and the like. The stilbeneglycoside has a wide application prospect on the aspects of health care and the like.
US8618101 N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
CN102617380A Carbonic acid diester water-soluble derivant of amino acid and propofol, and application of carbonic acid diester water-soluble derivant of amino acid and propofol The invention relates to a carbonic acid diester water-soluble derivant of amino acid and propofol, and application of the carbonic acid diester water-soluble derivant of amino acid and propofol. The amino acid carbonic acid diester of propofol has the structure which is shown as a formula (1), wherein R is shown in the specifications; and the invention also discloses a preparation method for the compound with the formula (I), pharmaceutical salt of the compound, a medical composition of the compound and the pharmaceutical salt of the compound, and application of the compound used as a dope.
CN103113375A Pyrazolo [3, 4-d] pyrimidine compounds and preparation method thereof The invention relates to pyrazolo [3, 4-d] pyrimidine compounds (shown in a formula I in the specification) and a synthesis method thereof. The raw materials in the route are easy to get, the steps are simple and the reaction yield is high. The invention further relates to an application of the compounds in treating cell hyperplasia diseases and autoimmune diseases.
CN103394078A Self-pressurized multi-target collaborative hemostasis degradable hemostatic preparation for injury first aid The invention discloses a self-pressurized multi-target collaborative hemostasis degradable hemostatic preparation for injury first aid. The self-pressurized multi-target collaborative hemostasis degradable hemostatic preparation comprises the following components in percentage by weight: 10-90% of a biodegradable material, 1-40% of thrombin, 1-40% of fibrinogen, 1-40% of coagulation factors, 1-20% of tranexamic acid, 1-20% of amine removing vasopressin, 0.5-20% of a calcium salt, 0.1-5% of a local anesthesia analgetic and 0.01-2% of nano silver. The hemostatic preparation is used for realizing hemostasis actively and passively, and promoting hemostasis from each link of a blood coagulation mechanism, so that bleeding can be controlled in a short time, and the hemostatic preparation is good in biocompatibility, degradable adsorption and safety.
US20100278902 Strontium doped bioactive glasses The invention relates to bioactive glasses containing or doped with strontium, to a method for preparing the same and to the use thereof in methods for bone repair or reconstruction.
CN102796153A Novel antitumor component Swertiridoid A in swertia phragmitiphylla The invention relates to a novel antitumor component Swertiridoid A in swertia phragmitiphylla. The molecular formula of the Swertiridoid A is shown as C16H20O10. The chemical structure of a compound is determined through multiple types of conventional spectrum analysis; the compound is iridoid glycoside of which the aglycone is similar to cantharidin, contains a sugar structure in molecules, and has high water solubility. Meanwhile, as proved by an in-vitro antitumor experiment, the compound has a remarkable inhibiting effect on tumor cell strains. A pilot compound can be provided for the research and development of novel antitumor medicaments, and plays an important role in developing and utilizing special plant medicinal materials on the Qinghai-Tibet Plateau.
WO2007013147A1 Angiogenesis inhibitor and vascular regressive agent Disclosed are a novel angiogenesis inhibitor and a novel vascular regressive agent. The angiogenesis inhibitor and the vascular regressive agent each comprise a 3,4-dihydroxyphenylalanine derivative such as N-β-alanyl-5-S-glutathionyl-3,4-dihydroxyphenylalanine, β-alanyl-3,4-dihydroxyphenylalanine and 5-S-cysteinyl-3,4-dihydroxyphenylalanine or a pharmaceutically acceptable salt thereof as the active ingredient.
US20110288151 Methods of characterizing breast cancer and identifying treatments for same This application describes antibodies to P-Rex 1, and methods of detecting breast cancer, and methods of treatments for the same.
US20110064796 Concentrated, inhalable antibiotic formulation A concentrated inhalable formulation of an antibiotic drug such as ciprofloxacin is disclosed. The antibiotic is formulated with sodium acetate and liposome which incorporate antibiotic. The formulation is aerosolized and inhaled for treatment of respiratory tract infections and other medical conditions.
CN101638391B 2-[(substituted aminobenzene)carbonylmethylthio]-6-(2,6-dichlorobenzyl)-3H-pyrimidyl-4-ketone derivative and preparation method and application thereof The invention provides a 2-[(substituted aminobenzene)carbonylmethylthio]-6-(2,6-dichlorobenzyl)-3H-pyrimidyl-4-ketone derivative with the general structure shown as follows, wherein, R1 is H or methyl; R2 is 4-chlorine, 4-methoxyl, 4-nitryl, 3,4-dichloro, 4-bromine, 3,4-difluoro, 3-chlorine-4-fluorin, 3,4-dimethoxy or 4- methyl. The invention also relates to a preparation method of the compound and application of the compound as an HIV inhibitor.
US20140005272 Administration of n,n-dimethylacetamide and its monomethylated metabolites for the treatment of inflammatory disorders The subject invention is directed to the treatment of inflammatory disorders by administration of N, N-dimethylacetamide and its mono-methylated metabolites. The compounds are useful in the management or treatment of inflammatory disorders, such as preterm birth and preterm labor, cardiovascular disorders, dermatologic diseases, musculoskeletal disorders, infection, autoimmune disorders, gastrointestinal disorders, pulmonary disorders, neurodegenerative disorders, genitourinary disorders, oncologic and endocrine disorders as well as inflammation associated with these and other disorders. The treatment may take a variety of forms and is intended for a variety of mammals, such as premature neonates to adult humans.
US20120277252 Antibacterial Agents and Methods of Use Thereof The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alkyl groups, and optionally having hydroxyl and/or alkoxyl groups substituents.
US7101863 For skin, muscle, ocular or gastric mucosal healing The invention concerns pharmaceutical compositions with wound healing or anti-complementary activity, and their uses, said compositions comprising, (1) at least a dextran derivative of general formula DMCaBbSuc, a, b, and c respectively representing the degrees of substitution in the groups MC, B and Su, wherein a≧0.6, b=0 or ≧0.1, and c=0 or ranges widely between 0.1 and 0.5 for a wound healing composition, and a≧0.3, b≧0.1 and c=0 or ranges widely between 0.1 and 0.4 for a composition with anti-complementary activity; (2) and at least a pharmaceutically acceptable carrier, said dextran derivative being present in a single unit dose or at a concentration adapted to the desired wound healing or anti-complementary activity.
WO2012051601A3 Heteroarylthio compounds Heteroarylthio compounds covalently linked to an arylpiperazine moiety for the treatment of neurological conditions.
US20130065946 Materials and Methods Related to Modulation of Mismatch Repair and Genomic Stability by miR-155 The present invention provides materials and methods related to modulation of mismatch and genomic stability by miR-155.
CA2190148C Oral liquid alendronate formulations Disclosed is a therapy protocol for treating and for preventing bone loss in patients who have difficulty in swallowing by administering a liquid formulation of alendronate which can be easily swallowed. Also described are pharmaceutical dosage forms of a syrup, aqueous solution, a solution formed from a reconstituted powder, of alendronate, for carrying out the therapeutic method.
CN1740187A Application of peininine and its derivative in preparing antitumor medicine The present invention discloses the application of peininine and its 3-position derivatives in preparing antitumor medicines. The peininine 3-position derivatives include 3bata-acetylated peininine, 3-oxidized peininine, 3beta-benzoylated peininine, 3beta-propionylated peininine, 3beta-butyrylated peininine and 3beta-butoxycarbonylated peininine. Peininine and its 3-position derivatives in different concentrations have inhibition effect on the proliferation of mouse H22 tumor cell and have excellent dose-effect relationship.
WO2006009755A3 Azaindoles modulating c-kit activity and uses therefor Compounds with 7-azaindole core structure with activity toward the receptor protein tyrosine kinase c-kit, compositions useful for treatment c-kit-mediate diseases or conditions, and methods of use thereof, are provided. Further provided are methods of c kit ligand identification and design.
WO2009109866A3 Intermediates and a process employing the intermediates for the preparation of (3-trifluoromethylsulfonyl)-n-[4-methyl-3- (4-pyridin-3-yl-pyrimidin-2ylamino)-phenyl]-benzamide This invention relates to a process for the preparation of (3-trifluoromethylsulfonyl)-N-[4- methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula (I)) starting from 4-methyl-2-nitro-aniline (formula (II)) through intermediates (3- trifiuoromethylsulfonyl)-N-[4-methyl-3-nitrophenyl]-benzamide (formula (III)), (3- trifluoromethylsulfonyl)-N-[3-amino-4-methylphenyl]-benzamide (formula (IV)) and (3- trifluoromethylsulfonyl)-N-[3-guanidino-4-methylphenyl]-benzamide (formula (V)). This invention also relates to processes for the preparation of these intermediates. The compound of formula (I), also known as AN-024, is: (I).
US20100256179 Combination therapy for pain in painful diabetic neuropathy A method for treating pain in painful diabetic neuropathy comprises administering in combination a first agent that comprises a compound as defined herein, illustratively lacosamide, and a second agent effective to provide enhanced treatment of pain, by comparison with the first agent alone. The second agent illustratively comprises an analgesic, an anticonvulsant, an antidepressant or an NMDA receptor antagonist.
EP1577294A4 S-substituted n-1- (hetero)aryl alkyl-n - (hetero)aryl alkylysothiocarbamides, method for the production thereof, physiologically active s-substituted n-1- (hetero )aryl alkyl-n - (hetero)aryl alkylysothiocarbamides,a pharmaceutical compound and curing method The invention relates to s-substituted N-1-[(hetero)aryl]alkyl-N′-1-[(hetero)aryl] alkylysothiocarbamides and the physiologically active salts and bases thereof, embodied in the form of racemic mixtures (or stereoisomer mixture) or individual optical isomers. The specific physiological activity of said compounds makes it possible to use them in the form of molecular tools . Said invention also relates to Pharmaceutical compositions, containing said compounds and to a method for preventing and curing various diseases including neurodegenerative diseases as, for example Alzheimer's disease (AD). The pharmacological effect of said compounds is based on the combined cognitive-stimulating and neuroprotective action thereof, which is produced by acting on chemo-controlled calcium channels of neurone membranes, in particular the neurones regulated by glutamate receptors of the central neural system (CNS).
US20060293322 For therapy of lung and breast cancer The present invention relates to a compound of Formula (I) and its use in treating hyper-proliferative disorders.
CA2646359A1 A carious-bacteria-kill nano-toothpaste The present invention refers to a carious-bacteria-kill nano-toothpaste. The present invention overcomes the defects of existing toothpaste that cannot kill the bacteria, and provides a safe, effective sterilizing, clean teeth and anticaries nano-toothpaste. In order to solve these technical problems, the invention of the nano-toothpaste contains nano scale titanium dioxide (TiO2), adhesives, vesicants, wetting agents and water, in which nano-titanium dioxide (TiO2) weights 0.1 to 50% of the total weight, its specialty rests with: it also contains the nano silver-containing fungicides weight 0.1 to 50% of the total weight. After the use of such technology, this invention, nano-toothpaste, has the function of teeth clean and sterilization. It can be used in prevent caries, toothache cure, and has therapeutic effect on per periodontitis, mouth ulcers and bad breath.
CN102145010A Use of combination of potassium and magnesium for preparing medicine for preventing or treating gout The invention relates to use of combination of potassium and magnesium for preparing a medicine for preventing or treating gout, wherein the potassium and the magnesium are in pharmaceutically acceptable salt form. The scheme of the invention can efficiently prevent or treat the acute gout with little toxic and side effects; therefore, the invention provides a new selection for preventing or treating the gout.
US8765789 2-pyridinecarboxamide derivatives The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
CN1814110A Medicine for treating gynecophathy The invention is a medicine for curing gynaopathy and the preparing method thereof, having characters of good solubility, high human biological utilization ratio, etc, and obtaining medicinal extracts from the eleven medicinal materials- Nutgrass Galingale Rhizome (prepared with vinegar), Rhizoma Chuanxiong, Chinese Angelica, Rhizoma Corydalis(prepared with vinegar), largehead atractylodes Rhizome, liquorice root, Chinese Date, White Paeony Root, Red Paeony Root, Rehmannia(Cooked), calcium carbonate, and making them together with dispersive medium, suspending aid, antiseptic and emulsifier into capsules; or making them together with filling agent, releasing agent, wetter and lubricant into dispersive tablets; or making them into other oral preparations. The process research shows that the peony glucoside content of the medicine can be higher in the accelerated stability test.
EP1572675B1 New alpha-glucosidase inhibitors and their synthesis from a natural source The present invention provides novel a-glucosidase inhibitory compound (-)-mesquitol and its analogs isolated in significant yield from traditional medicinal plant Dichrostachys cinerea and further modification of (-)-mesquitol to enhance the a-glucosidase inhibitory potential; the invention also identifies the usage of (-)-mesquitol and its analogues, based on their a-glucosidase inhibitory activity, as broad based potential therapeutics as antihyperglycemic, antidiabatic, antiobesity, antiviral, anticancer, immunestimulants and the like.
US20090149498 Pharmaceutical composition having prokinetic effect The invention refers to the use of O-(3-piperidino-2-hydroxypropyl)nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof for the preparation of a pharmaceutical composition that restores and/or enhances the activity of the neuronal nitric oxide synthase enzyme.
US20050124632 Use of aminobenzenesulfonic acid derivative or a salt, hydrate, or solvate thereof; treatment of heart failure or arrhythmia in diabetic ischemic heart disease An agent for therapeutic and/or prophylactic treatment of heart failure or arrhythmia in diabetic ischemic heart disease, which comprises as an active ingredient an aminobenzenesulfonic acid derivative represented by the following general formula (I): (wherein R1 represents, for example, hydrogen atom; R2 represents, for example, hydrogen atom; and n represents an integer of from 1 to 4) or a salt thereof, or a hydrate thereof or a solvate thereof, and an agent for therapeutic and/or prophylactic treatment of diabetic ischemic heart disease wherein said agent improves a cardiac dysfunction in diabetic ischemic heart disease.
US20110274778 Use of a compound comprising D-mannoheptulose and/or perseitol for treating and preventing innate immunity modification diseases The invention relates to the use of a compound comprising D-mannoheptulose and/or perseitol for producing a drug for treating and/or preventing diseases related to the modification of an innate and/or acquired immunity by increasing the production of antimicrobial peptides, preferably hBD-2 without inducing inflammatory reactions, irritation or intolerance. Said compound can also comprise a peptidic avocado extract an/or a peptidic lupin extract.
EP1325745B1 Preventives and remedies for complications of diabetes Preventives and remedies for complications of diabetes which contain as the active ingredients compounds represented by the following general formula (1) or lactone derivatives thereof: (1) wherein R represents an organic group; X represents CH2CH2- or CH=CH-; and M represents hydrogen, C1-10 alkyl or a physiologically acceptable cationic group. These drugs are useful in preventing and treating complications of diabetes such as diabetic nephropathy, diabetic neuropathy, diabetic retinopathy and diabetic angiopathy.
CN1820749A Formula of amoxycillin sodium/ambroxo/ hydrochloride powder injection and its preparing method The present invention provides a recipe and preparation of amoxicillin sodium/ambroxol hydrochloride powder for injection. The amoxicillin sodium/ambroxol hydrochloride powder for injection contains amoxicillin sodium and ambroxol hydrochloride in the ratio of 25-100 to 1-5, preferably 50 to 3. The present invention is superior to orally taken amoxicillin sodium/ambroxol hydrochloride preparation, which has the demerits of low bioavailability, slow acting and more side effect on gastrointestinal tract. The amoxicillin sodium/ambroxol hydrochloride powder for injection has determined curative effect, and is especially suitable for serious patient and children patient without automatic respiration, auto expectoration and difficult medicine taking.
CN101095744A Exterior-applied medicine for treating scald and the method for preparing the same Disclosed is an externally-applied medicament for treating scalds and its preparing process, wherein the medicament is prepared from the following raw materials (by weight portion): alum 25-30g, pricklyash peel 6-8g, sesame oil 8-10g. The invention realizes simplified treatment, low cost, quick effect, non-irritation, and no side effects.
CN102657634A Nifuroxazide microcapsule powder and production method thereof The invention discloses nifuroxazide microcapsule powder and a production method thereof. The nifuroxazide microcapsule powder is characterized by consisting of nifuroxazide, n-cyclohexylsulphamic acid, silicon dioxide micro powder and polyethylene glycol in a weight ratio of 1: (0.01-0.02): (1-3): (3-6). The production method comprises the following steps of: dissolving the n-cyclohexylsulphamicacid by using 95 percent ethanol, stirring with fine nifuroxazide powder to wet the fine nifuroxazide powder uniformly, adding the silicon dioxide micro powder to form a core material, mixing the core material and the polyethylene glycol 4000 or polyethylene glycol 6000 uniformly, performing interlayer heating at the temperature of between 75 and 80 DEG C to melt the mixture, cooling, curing, drying, crushing with airflow to form powder with the particle diameter of 90 to 100 meshes, and thus obtaining the nifuroxazide microcapsule powder. The nifuroxazide microcapsule powder is low in heat loss rate and high in flowability, has a good feeding effect, and facilitates industrialized production.
US7371753 Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.
CN101337967A Mouth cavity articles, preparation method thereof and applications thereof The invention discloses a G(Mulberrofuran G) compound, a preparation method and the application thereof for preparing drugs for treating or preventing oral diseases and preparing oral care products.
EP2035425A1 Amino- imidazolones and their use as a medicament for treating cognitive impairment, alzheimer disease, neurodegeneration and dementia. This invention relates to novel compounds having the structural formula I below and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
CN1600305A Oral liquid prepared-from extractive of ginkgo leaf for anti heart and cerebral ischemia, and reducing blood fat and for enhancing memory A heath-care food in the form of oral liquid for preventing cardiac and cerebral ischemia, improving blood circulation and memory, decreasing blood fat and viscosity and softening blood vessel is prepared from the extract of ginkgo leaf, honey, haw powder and purified water through proportionally mixing.
US20080293619 Compositions and methods for treating malaria with cupredoxin and cytochrome The present invention relates to cupredoxin and cytochrome and their use, separately or together, to inhibit the spread of parasitemia in mammalian red blood cells and other tissues infected by the malaria parasite, and in particular the parasitemia of human red blood cells by P. falciparum. The invention provides isolated peptides that are variants, derivatives or structural equivalents of cupredoxins or cytochrome c, and compositions comprising cupredoxins and/or cytochrome c, or variants, derivatives or structural equivalents thereof that are useful for treating or preventing malaria infection in mammals. Further, the invention provides methods to treat mammalian patients to prevent or inhibit the growth of malarial infection in mammals. The invention also provides methods to prevent the growth of malaria infection in insect vectors.
CN103446060A Docetaxel polydroxybutyrate nanoparticle, manufacturing method and pisum sativum agglutinin modification method and application The invention discloses a docetaxel polydroxybutyrate nanoparticle, a manufacturing method and apisum sativum agglutinin modification method and application. The manufacturing method of the docetaxel polydroxybutyrate nanoparticle includes the steps that docetaxel and thichloromethane and/or dichloromethane of polyhydroxybutyrate are uniformly mixed and then mixed with an aqueous solution of polyvinyl alcohol, then ultrasonic emulsification is carried out for 3-10 min, curing is carried out, and organic solvents are removed; the mass ratio of the docetaxel to the polyhydroxybutyrate to the polyvinyl alcohol is (0.8-2): (4-10): (20-50). The solubility of the docetaxel is improved, distribution of particle sizes of manufactured products is even, the quantity of carried drugs is large, the packing rate is high, drug release is quick, drugs are released in a controlled mode out of the body, and the bioavailability is high. The docetaxel polydroxybutyrate nanoparticle undergoing apisum sativum agglutinin modification improves drug targeting performance and treatment indexes, and lays a foundation for development of a tumor targeting drug delivery system mediated by specific sugar.
CN101278950A Externally used ointment for curing empyrosis and method of producing the same The invention discloses an external-use paste used for treating burn and scald and a preparation method thereof. The weight proportion of material composition of effective components of the invention are plaster of paris, burnt lime, sesame oil, dog bone coal, borneol and sulphanilamide crystal. The preparation method is as follows that calcium sulfate is put into an earthen pot and is covered by an iron covering, and then the earthen port is put into smokeless fire to be calcined; after being cooled, plaster is taken out, levigated into power and sieved by a bolter; lime is put into the earthen pot and is covered by the covering, and then the earthen port is put into the smokeless fire to be calcined; after being cooled, the plaster is taken out, levigated into power and sieved by the bolter; the dog bone is put into the smokeless fire to be calcined; after being cooled, the dog bone is taken out, levigated into power and sieved by the bolter; the sulphanilamide crystal and borneol are levigated into power; and the above various drugs are mixed together in proper proportion and are mingled into the paste by adding the sesame oil. The paste is applied to the surface of a wound several times per day with small brush. As long as the paste is dry, the paste can be applied again. The external-use paste of the invention has the functions of improving anti-infectious ability, inhibiting exudation and quickly stopping pain. In addition, granulation can grow quickly and no scar is left when the surface of the wound is healed up.
US20070219209 Piperazine Derivatives Of Alkyl Oxindoles The present invention is concerned with new indol-2-one derivatives of the general Formula (I). The new compounds are useful for the treatment or prevention of the disorders of the central nervous system or the cardiovascular system.
CN102370744A Formula for improving cervical spondylosis and osteoarthrosis A formula for improving cervical spondylosis and osteoarthrosis comprises the following components, by weight: 1-5 parts of D-glucosamine, 15-20 parts of root of kudzu vine, 45-50 parts of pawpaw and 30-35 parts of haw. The invention is characterized in that raw materials are selected from natural plants both for medicine and food, such as root of kudzu vine, pawpaw and haw, and companied with D-glucosamine; the formula has no side effect and has effects of improving spondylosis and osteoarthrosis, and is suitable for the group with osteoarthritis family history, the group of joint excessive usage for a long term, the overweight, the group older than 65, computer worker, white collars and drivers, and especially has good preventive and treatment effect on middle aged and old people and people with excessive cervical vertebra usage.
CN1562022A Compound for treating leukemia and multiple myeloma A compound, lycozine, for treating leukemia and multiple myeloma is disclosed. It can be applied individually or in conjunction with other medicines.
CN1795862A Gelata of ValaciclovirHydrochloride A gel of valaciclovir hydrochloride for treating varicella-zoster by exterior application is prepared through dissolving valaciclovir hydrochloride in alkaline aqueous solution to obtain its alkaline solution, mixing the gel matrix with solvent, stirring, regulating pH=6-10, adding surfactant (polysorbate 80), stirring, and respectively adding said alkaline solution, antiseptic agent, and distilled water while stirring.
CN102311416A Hydroxy substituted flavonoid compound, preparation method and application thereof The invention discloses a hydroxy substituted flavonoid compound, a preparation method and application thereof. The hydroxy substituted flavonoid compound has a structural formula shown as a formula (I). An effect of enhancing an ABA1 promoter activity of the hydroxy substituted flavonoid compound of the invention is obviously better than that of an existing positive medicament GW3965; and a dosage is small. The hydroxy substituted flavonoid compound can be applied to preparation of medicaments for treating lipid metabolism disorder, especially medicaments for treating atherosclerosis and senile dementia, with good effects, and has a wide application prospect.
EP0991638B1 NOVEL GUANIDINE MIMICS AS FACTOR Xa INHIBITORS The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.
CN103709172A Substituted furan-piperidine derivative and application thereof The invention relates to the biological medicine field, and specifically relates to a substituted furan-piperidine derivative and an application thereof. The compound has a structure shown as a general formula (I). The invention also provides an application of the substituted furan-piperidine derivative as a Janus kinase inhibitor. The formula (I) is shown in the description.
EP1676577A1 Compositions for the treatment of cancer comprising a topoisomerase inhibitor and thalidomide This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a pharmaceutically acceptable salt, solvate, or clathrate thereof, and irinotecan. The invention also relates to methods of treating or preventing cancer which comprise the administration of a thalidomide and another anti-cancer drug to a patient in need of such treatment orprevention. The invention further relates to methods of reducing or avoiding adverse side effects associated with the administration of chemotherapy or radiation therapy which comprise the administration of thalidomide to a patient in need of such reduction or avoidance.
CN101406477A Application of Breviscapine in preparing medicine The invention discloses application of breviscapine in preparing drugs. The breviscapine has the functions of increasing fetal blood oxygen partial pressure (pO2) and the blood oxygen saturation (SO2 percent) and reducing the fetal blood carbon dioxide partial pressure (pCO2) so that pregnancy uterine arteries are diastolic obviously. The prepared drugs are used for treating or preventing intrauterine fetal ischemia and hypoxia.
EP2486060A1 Siglec 15 antibodies in treating bone loss-related disease Novel antibodies and antigen binding fragments that specifically binds to Sιglec-15 are described herein In some embodiments, the antibodies or antigen binding fragments may block the biological activity of Sιglec-15 and are useful in composition for the treatment of bone loss, more particularly in bone diseases that have increased cell surface expression of Sιglec-15, such as conditions where there is an increase in the bone degradative activity of osteoclasts The invention also relates to cells expressing the antibodies or antigen binding fragments such as monoclonal, humanized or chimeric antibodies Additionally, methods of detecting and treating bone loss, bone-related diseases or cancer using the antibodies and fragments are also disclosed.
WO2007078007A1 Carbon nanohorn structure, composition capable of controlling the release of organic substance included therein, and method for the controlled release Disclosed is a carbon nanohorn structure wherein an oxygen-containing functional group located at an open edge of the nanohorn is bound to a cation. Also disclosed is a carbon nanohorn structure having an organic substance included in an internal space of the nanohorn. A novel carbon nanohorn structure is provided which can control the release of a substance included therein through an opening site precisely by a simple means. By employing the carbon nanohorn structure, it becomes possible to provide a novel means for achieving the controlled release of a substance included in the carbon nanohorn structure.
US20110207692 Combinations of sapacitabine or cndac with dna methyltransferase inhibitors such as decitabine and procaine A first aspect of the invention relates to a combination comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to a subject.
CN103405383A Clindamycin phosphate gel and preparation method thereof The invention discloses a clindamycin phosphate gel and a preparation method thereof. The gel contains the active component clindamycin phosphate and adjuvant materials, wherein the adjuvant materials comprise hydroxy propyl cellulose and phosphatidylcholine. According to the invention, a phosphatide compound is prepared from clindamycin phosphate, so hydrolysis of clindamycin phosphate is prevented in virtue of protection of drugs by phosphatidylcholine, and the prepared gel has good stability and is convenient for transdermal absorption; the gel hardly undergoes layering and is easy to coat.
US7214676 Spirotricyclic derivatives and their use as phosphodiesterase-7 inhibitors The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are as defined in the description, methods for preparing them and their use for the treatment of disorders for which therapy by a PDE7 inhibitor is relevant.
WO2013107285A1 Amino heteroaryl compound, preparation method therefor and use thereof The present invention provides amino heteroaryl compound represented by the following formula (I), preparation method therefor and use thereof, wherein the definitions of R1 and R3 are described detailedly in the description. The amino heteroaryl compound of the present invention is hepatocyte growth factor receptor (c-Met) inhibitor, having good inhibition effect of c-Met and cancer cell proliferation, thus can be used as a therapy agent for treating tumor and related diseases.
WO2005002583A1 Use of thieno`2,3-d ! pyrimidines for the prophylaxis or treatment of hyperactivity disorder In order to develop a method for the prophylaxis or treatment of hyperkinetic disorders or attention-deficit/hyperactivity disorder, the present invention offers a thieno[2, 3-d]pyrimidine derivative, an optical isomer thereof, a medicinally acceptable salt, a hydrate thereof or a solvate thereof.
CN101926776A Salinomycin sodium suspension as well as preparation method and application thereof The invention discloses a salinomycin sodium suspension as well as a preparation method and an application thereof. The salinomycin sodium suspension comprises the following components in parts by weight: 2-30 parts of salinomycin sodium, 20-90 parts of filler, 5-40 parts of flavoring agent, 2-20 parts of suspending agent and 1-30 parts of wetting agent. The preparation method of the salinomycin sodium suspension comprises the following steps: sieving and mixing all raw materials, adding the wetting agent to prepare soft material, drying and pelletizing to obtain the product in the invention. The salinomycin sodium suspension in the invention has evenly distributed particles, high bioavailability, rapid drug response, simple preparation process and wide application prospect, and can become a liquid preparation after water is added.
WO2012006060A1 Compounds and methods for the treatment or prevention of flavivirus infections A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
US6998426 Oil in water emulsion These objects and others may be accomplished with the present invention, the first embodiment of which provides an oil-in-water nanoemulsion, which includes: an oily phase dispersed in an aqueous phase; (i) at least one amphiphilic lipid selected from the group including nonionic amphiphilic lipids, anionic amphiphilic lipids, and combinations thereof; and (ii) at least one water-soluble nonionic polymer selected from the group including homopolymers and copolymers of ethylene oxide; polyvinyl alcohols; homopolymers and copolymers of vinylpyrrolidone; homopolymers and copolymers of vinylcaprolactam; homopolymers and copolymers of polyvinyl methyl ether; neutral acrylic homopolymers and copolymers; C1–C2 alkyl celluloses and their derivatives; C1–C3 alkyl guar; C1–C3 hydroxyalkyl guar; and combinations thereof; wherein a ratio of the weight of the oily phase to the weight of the amphiphilic lipid (i) ranges from 1.2 to 10; and wherein the oily phase includes oil globules having a number-average size of less than 100 nm. The nanoemulsion obtained is preferably transparent and stable on storage. It may form a composition for topical, preferably cosmetic or dermatological compositions, pharmaceutical compositions and ophthalmological compositions.
EP2614711A1 Disinfectant and/or bactericidal aqueous compositions The present invention provides a disinfectant and/or bactericidal aqueous composition containing an olanexidine acid addition salt and a cyclodextrin.
WO2006073151A1 Novel fermentation product A novel cyclic compound, which is isolated from novel Streptomyces sp. Q34752 strain and Q47152 strain, shows an excellent antibacterial activity against bacteria of the genus Propionibacterium, in particular, Propionibacterium acnes and so on. Thus, it is useful as an antibacterial agent for treating acne vulgaris. Moreover, the above compound has a favorable antiinflammatory activity and, therefore, is useful in preventing or treating various inflammatory diseases. The novel strains producing this compound and a method of producing this compound by using these strains are also provided.
CN102250022A Substituted quinoxalinamine compounds, and preparation method and application thereof The invention provides N-substituted-3-substituted quinoxaline-2-amine compounds. Quinoxaline compounds are taken as precursors, different substituted amino groups and aryl groups are introduced into the second positions and the third positions of parent nuclei of quinoxalines, and the N-substituted-3-substituted quinoxaline-2-amine compounds are synthesized. Pharmacological tests prove that the compounds and salts thereof have obvious activity of inhibiting tumor cells in vitro, and the IC50 reaches the mu M level; and the pharmacological tests indicate that the antitumor activity of the compounds is related with the inhibition of the compounds on a PI3K/Akt signal path. The design is reasonable, the preparation method is simple and convenient and suitable for practice, and the compoundscan be applied to preparation of antitumor medicines. The structural general formula of the compounds is shown as the specifications.
WO2013102655A1 4,4-disubstituted-1,4-dihydropyrimidines and the use thereof as medicaments for the treatment of hepatitis b Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1-R5, B and Z have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.
CA2574623C Acidic solid oral compositions without erosive potential in saliva and method for determining erosive potential in saliva Acidic oral compositions having calcium contents and effective pH-values in the area indicated by grey~ tone in Fig. 2 are non-erosive in saliva and capable of stimulating saliva production, even in "dry mouth" patients. A new multi-step test method for determin~ing erosive potential in saliva has been used for identifying the compositions.
CN103251559A Combretastatin A-4 atomization agent and preparation method thereof Combretastatin A-4 is effective in treatment of thyroid cancer, ovarian cancer and lung cancer, a monotromethamine salt preparation of combretastatin A-4 phosphate is applied during clinical medication, a phosphate salt prodrug is hydrolyzed in vivo into combretastatin A-4 to work, but the phosphate salt prodrug has adverse reactions, such as transitory electrocardiogram change, hypertension and arrhythmia. Combretastatin A-4 is prepared into an atomization agent which can be inhaled into the lung, thus the cost of synthesizing a prodrug is reduced, meanwhile, the adverse reactions brought by the prodrug are overcome, and more importantly, the action of local administration on the lung is achieved. Solvents water, 1,2-propanediol, dimethylsulfoxide, N,N-dimethylformamide, ethanol and tert-pentylalcohol which are used for dissolving combretastatin A-4 are common medicament auxiliary materials. When a solution is added into an ultrasonic atomizer or an electronic cigarette for atomization, a combretastatin A-4 atomization agent is obtained.
US20110046094 Methods and compositions for identifying and treating lupus A unique set of genetic variations associated with lupus are provided. Also provided are methods for detecting such genetic variations and for assessing risk of developing lupus as well as for diagnosing and treating lupus.
CN101926812A New application of apigenin-7-O-beta-D-glucoside-4'-O-alpha-L-rhamnoside The invention discloses a new application of apigenin-7-O-beta-D-glucoside-4'-O-alpha-L-rhamnoside in preparing medicines or healthcare food for the prevention and the treatment of gastric precancerous lesion, in particular, intestinal metaplasia and/or atypical hyperplasia of gastric mucosa.
WO2011122321A1 Agent for inhibiting physiological activity of heparin-binding protein The purposes of the present invention are to elucidate the physiological importance of glycosaminoglycans such as heparin and heparan sulfate and to provide novel applications of these molecules. Specifically disclosed is an agent for inhibiting the physiological activity of a heparin-binding protein, which contains a sulfated saccharide as an active ingredient. The agent for inhibiting the physiological activity of a heparin-binding protein is utilized, for example, as an angiogenesis inhibitor.
CN101953787A Tablet containing cefprozi liposome and preparation method thereof The invention relates to a cefprozi liposome, a preparation method thereof and a tablet containing the cefprozi liposome. The cefprozi liposome comprises cefprozi, hydrogenated soybean phosphatidylcholine, hydrogenated egg yolk lecithin and cholesterol, wherein the weight ratio of the cefprozi, the hydrogenated soybean phosphatidylcholine, the hydrogenated egg yolk lecithin and the cholesterol is 1:1.25-5:1.25-5:2.5-10. The cefprozi tablet meets the requirements of Chinese Pharmacopoeia and also has the advantages of higher dissolution rate, faster effect and greatly enhanced bioavailability compared with the ordinary cefprozi drug composite.
CN101199518A Paediatrics amoxicillin Na dissolve sheet The invention relates to an amoxicillin sodium soluble tablet with special specification for children, comprising effective amount of amoxicillin sodium and water-soluble medicinal excipient which disintegrates fast to release efficacy in water. When the patient takes the tablet, the patient can determine the taken number of the tablets according to the body weight of the patient. Thus, personalized administration can be realized; the medicine intake can be more accurate; and the safety is higher. After the medicine is dissolved in the water, the water can become a sweet and sour beverage, so the taken method is more acceptable by children with good compliance. At the same time, the medicine solution is easy to be fully absorbed by the body , and the bioavailability is higher.
CA2181073C Tissue-specific enhancer active in prostate The invention provides a human prostate-specific transcriptional regulatory sequence, polylnucleotide comprising such regulatory regions, toxin gene constructs wherein a toxin gene is expressed under the transcriptional control of a human prostate-specific transcriptional regulatory sequence, and methods for treating prostate disease using such toxin gene constructs.
US7087643 Side effect reduction of diabetes, strokes, multiple sclerosis This invention is directed to a method for preventing or treating neuropathic pain and cluster and migraine headache-associated pain comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I): wherein phenyl is substituted at X with one to five halogen atoms independently selected from the group consisting of fluorine, chlorine, bromine and iodine; and; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1–C4 alkyl; wherein C1–C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of hydrogen, halogen, C1–C4 alkyl, C1–C4 alkoxy, amino, nitro and cyano).
CN101019869B Medicine composition of alprostadil and Chuanhuning/Yanhuning liposome and its preparation The present invention relates to medicine composition of alprostadil and Chuanhuning/Yanhuning liposome and its preparation process. The nanometer liposome medicine contains the mixture of alprostadil and Chuanhuning/Yanhuning in the weight ratio of 0.1-1.0 to 50-300 in 10.1-80.2 weight portions, the mixture of soybean lecithin and yolk lecithin in the weight ratio of 4 to 1 in 88-440 weight portions, the mixture of cholesterol and beta-sitosterol n the weight ratio of 9 to 1 in 40-200, polyethylene glycol in 4000 15-40 weight portions, sodium glucuronate in 100 -280 weight portions and vitamin C in 160-800 weight portions. The medicine of the present invention may be used in antagonizing pneumonia adenovirus and influenza virus.
EP2001475A2 Methods for treating sarcopenia with a growth hormone secretagogue The present invention relates to methods for treating sarcopenia with a growth hormone secretagogue.
CA2399293C Optically-active nanoparticles for use in therapeutic and diagnostic methods This invention is generally in the field of improved methods for the localized delivery of heat and the localized imaging of biological materials. The delivery may be in vitro or in vivo and is useful for the localized treatment of cancer, inflammation or to other disorders involving overproliferation of tissue. The method is also useful for diagnostic imaging. The method involves localized induction of hyperthermia in a cell or tissue by delivering nanoparticles to said cell or tissue and exposing the nanoparticles to an excitation source under conditions wherein they emit heat.
CA2247336C Parapoxviruses containing foreign dna, their production and their use in vaccines The present invention relates to recombinantly prepared parapoxviruses which carry, in their genomes, deletions or insertions in the form of foreign hereditary information and contain hereditary information, to the preparation of such constructs and to their use in vaccines.
US7642284 Luminacin analogs and uses thereof The present invention provides compounds having formula (I) (and pharmaceutically acceptable derivatives thereof): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R14 and n are as defined herein.
US20050059658 N-(2,4-Difluorophenyl)-N'-[3-(4,4-dimethyl-6-oxo-1,4,5,6-tetrahydro-3-pyridazinyl)-phenyl]urea and intermediates; antiviral The invention relates to novel compounds, to a method for the production of said compounds and to the use thereof as medicaments, more particularly as antiviral agents, especially against cytomegalovirus.
CN102961358A Abiraterone acetate liquid capsule The invention relates to an abiraterone acetate liquid capsule, comprising a capsule shell and contents, wherein the contents contain the components in percent by weight: 8-25% of abiraterone acetate and 74.8-91.8% of oil phase, wherein the oil phase comprises fatty acid monoglyceride and a solvent in a ratio of 1: 4 to 4: 1 by weight. The capsule disclosed by the invention does not contain a surfactant, as well as is good in dissolution rate, high in safety and simple in preparation process.
CN102920676A Celecoxib chewable tablet and preparation method thereof The invention provides a celecoxib chewable tablet and a preparation method thereof. The celecoxib chewable tablet consists of the following raw materials in percentage by weight: 5-30% of celecoxib, 5-20% of disintegrating agent, 20-80% of filler, 5-30% of adhesive, 0.5-5% of flow aid and 0.5-3% of surfactant. The celecoxib chewable tablet has the advantages of both tablets and fluid preparations and has the characteristics of even dispersion, very short disintegrating time limit, fast medicament dissolution and high bioavailability, and is better convenience to take. The celecoxib chewable tablet is especially suitable for the aged and the patients who have swallowing difficulties. Upon inspection, the celecoxib chewable tablet shows that the quality indexes such as content, characteristics, identification, disintegrating time limit and dissolution accord with the 2010 edition of China Pharmacopoeia and relevant regulations. The bioavailability of the celecoxib chewable tablet is higher than the tablets on sale.
US20090005356 Substituted pyrrolopyridines and pyrazolopyridines as kinase modulators Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis.
CN101103995B Application of fly maggot chitosan in preparing product regulating blood sugar The invention discloses an application of flyblow chitosan in the preparation of a product for regulating blood-sugar, in particular to an application in the preparation of medicine or a health product for preventing or treating diabetes. Compared with the prior art, the flyblow chitosan used in the invention is prepared from flyblow chitin; the chitin contained in the skin of a flyblow is more than that contained in the shell of a shrimp or crab while the carbonate, heavy metal and coloring matter in the skin of the flyblow is less than that in the shell of the shell of the shrimp or crab, therefore the quality of the flyblow chistosan is far better than chitin in the shell of the shrimp or crab; the flyblow chitosan not only has the function of reducing blood-sugar and improving sugar tolerance, without influencing normal glycometabolism but also has the advantages of non-immunogenicity, degradation in an organism, non-toxicity, no-production of transformation reactions, mild immunologic stimulation and influence to the organism and easiness for preparation; thus the flyblow chitosan has good application prospect as the medicine or health product for regulating blood-sugar, preventing and treating diabetes.
US20100057047 Delivery device and method A nasal delivery device for and method of delivering substance to the middle meatus in a nasal cavity of a subject in the treatment of a condition, in particular an inflammatory or infectious condition, thereof, the delivery device comprising: a nosepiece unit (17) including a nosepiece (20) for fitting to a nostril of a subject and a nozzle (25) through which substance is in use delivered to the respective nasal cavity; and a delivery unit (29) for delivering substance through the nozzle of the nosepiece; wherein the delivery device is configured to provide for deposition of a significant fraction of the delivered dose on, around and in the vicinity of the middle meatus.
WO2008082948A3 Ophthalmic alginate composition related methods of manufacture and methods of use The present invention is directed to an ophthalmic composition comprising alginate having a minimum of about 0 % and a maximum of about 50 % guluronic units bound to an adjacent guluronic unit as a percentage of the total number of monomelic units in the alginate. The composition further includes a cationic antimicrobial agent. The alginate set forth above forms less deactivating complexes with cationic antimicrobial agent, and thus, the composition has improved preservative efficacy.
CN101874779A Fructose diphosphate sodium liposome solid preparation and novel application thereof The invention provides a fructose diphosphate sodium liposome solid preparation and a novel application thereof. The fructose diphosphate sodium liposome solid preparation is prepared from fructose diphosphate sodium liposome and auxiliary materials, wherein the fructose diphosphate sodium liposome is prepared from fructose diphosphate sodium, lecithin, cholesterol and polyglycerin ester. The invention also provides the application of the fructose diphosphate sodium liposome solid preparation in improving the immunity of tumor patients undergoing chemotherapy. The fructose diphosphate sodium liposome can be prepared by adopting a thin-film dispersion technology to combine a certain amount of the lecithin, the cholesterol, the polyglycerin ester and the active component fructose diphosphate sodium, and is mixed with a certain amount of the auxiliary materials to prepare various solid preparations, so the invention can well solve the problems of poor in-vivo absorption degree and low curative effect, and obtains satisfactory technical effect.
CN103142549A Mannose ester enteric capsule and preparation method thereof The invention discloses a mannose ester enteric capsule and a preparation method of the mannose ester enteric capsule. The mannose ester enteric capsule is prepared by placing mannose ester enteric micropelets into a capsule shell, wherein the mannose ester enteric micropelets are composed of mannose ester micropelets and enteric coatings, wherein the enteric coatings are wrapped outside the mannose ester micropelets; the mannose ester micropelets consist of mannose esters and fillers; the enteric coatings are composed of enteric materials, plasticizers and antisticking agents; and when in preparation, the enteric coatings are wrapped outside the mannose ester micropelets so as to obtain the mannose ester enteric capsule. The mannose ester enteric capsule is convenient to take and ideal in enteric effect, and can improve the bioavailability; in addition, the preparation process is simple, the obtained product is stable in quality, and massive production and application can be realized.
US20110301104 Transition state structure of orotate phosphoribosyl transferases and uses thereof Methods are provided for designing a transition state inhibitor of orotate phosphoribosyltransferase (OPRT) and for inhibiting OPRT.
US20120316222 NOVEL RNAi THERAPEUTIC FOR TREATMENT OF HEPATITIS C INFECTION Small interfering RNAs (siRNAs) or small hairpin RNA (shRNAs) and compositions comprising same are provided that target human cyclophilin A (CyPA) to inhibit Hepatitis C (HCV) infection. Such siRNA and shRNAs may have a length of from about 19 to about 29 contiguous nucleotides corresponding to a specific region of human cyclophilin A (CyPA) cDNA of from about nucleotide 155 to about nucleotide 183 having particular potency against CyPA and HCV. Such siRNA and shRNAs may be formulated as naked compositions or pharmaceutical compositions. DNA polynucleotides, plasmids, and viral or non-viral vectors are provided that encode siRNA or shRNA molecules, which may be delivered directly to cells or in combination with delivery agents, such as lipids, polymers, encapsulated lipid particles, such as liposomes. Methods for treating, managing inhibiting, preventing, etc., HCV infection using such siRNA and shRNAs and compositions comprising same are also provided.
WO2010015870A1 Use of dihydralazine for the treatment of diseases related to elevated semicarbazide sensitive amine-oxidase (ssao) activity The present invention relates to the use of dihydralazine for the treatment of diseases related to elevated level of SSAO activity and its use for the manufacture of pharmaceutical compositions for the treatment of such diseases.
US20050123576 Mupirocin compositions for topical use, an improved process of making same and methods of using same Spreadable pharmaceutical compositions containing hard fat and Mupirocin, an improved process of preparing same and methods of using same are provided.
CN101708204A Medicinal composition for treating cardio-cerebrovascular diseases The invention discloses a medicinal composition for treating cardio-cerebrovascular diseases, which comprises the following raw materials in percentage by weight: 0.1 to 99.8 percent of ginkgo biloba P.E; 0.1 to 99.8 percent of sanchi extract; and 0.1 to 99.8 percent of aspirin. By utilizing the synergistic action of the ginkgo biloba P.E, the sanchi extract and the aspirin, the medicinal composition can effectively improve cardio-cerebrovascular circulation after the cerebral infarction and the miocardial infarction, dilate cardiac and cerebral vessels, and increase cardio-cerebral blood flow volume, and also can effectively improve microcirculation and reduce damage caused by ischemia-reperfusion after the cerebral infarction and the miocardial infarction.
US7390884 Lymphoid chemokines in the diagnosis, monitoring and treatment of inflammatory disease Experimental autoimmune encephalomyelitis (EAE) is a Th1-mediated autoimmune disease of the central nervous system that is widely used as an animal model of multiple sclerosis (MS). In this study it was demonstrate that CXCL13, a chemokine involved in the development of secondary lymphoid tissues, is expressed in CD11c+ myeloid cells that accumulate in EAE lesions. Blockade or deficiency of CXCL13 ameliorates clinical EAE, both during acute and relapsing stages. CXCL13 deficiency did not inhibit the priming or differentiation of autoimmune effector T-cells in the periphery, but appeared to exert its effects during the effector phase of pathogenesis. These findings indicate that reagents that antagonize or inhibit CXCL13 are useful for the treatment of neuroinflammatory diseases such as MS.
WO2011029088A2 Preparation of raloxifene and its salts The invention provides processes for the preparation of pure raloxifene or its salts, involving hydrolyzing 6-methylsulfonyloxy-2-[(4-methylsulfonyloxy)-phenyl]-3-[4(2-(piperidinyl)ethoxy)benzoyl]benzothiophene hydrochloride, using an aqueous base.
CN103751092A Valnemulin hydrochloride enteric solid dispersion, as well as preparation method and application thereof The invention belongs to the technical field of special antibacterial preparations for animals, and discloses a valnemulin hydrochloride enteric solid dispersion, as well as a preparation method and application thereof. The preparation method comprises the concrete steps of dissolving valnemulin hydrochloride and an enteric carrier in an organic solvent, and preparing a mixed liquid product by a solvent method; removing the organic solvent by using a rotary evaporator; grinding and screening to obtain the valnemulin hydrochloride enteric solid dispersion. The valnemulin hydrochloride enteric solid dispersion prepared by the method can be used for preparing special antibacterial premixes for animals. The preparation method is low in raw material cost and simple in production equipment and process operation; the prepared valnemulin hydrochloride enteric solid dispersion is stable in property, good in uniformity and large in mobility, does not have pungent smell or hygroscopicity, and is hardly released in an acid medium and almost completely released in a buffer salt medium.
US7476692 useful for the treatment of cancer and other hyperproliferative disorders; a sphingolipid; lactic acid; and optionally a stabilizing agent; emulsion The present invention provides stable aqueous solutions consisting essentially of: (a) a sphingolipid; (b) lactic acid; and (c) optionally a stabilizing agent; wherein the solution has a molar ratio of lactic acid to sphingolipid of 1:1 to 10:1. The present invention further provides an emulsion formulation consisting essentially of: (a) lactic acid; (b) a sphingolipid, wherein the sphingolipid is present in an amount of about 0.1 to about 30 mg/ml of emulsion; (b) optionally an isotonic agent; and (c) a phospholipid present in an amount of about 0.2 to about 200 mg/ml of emulsion. Methods of making and using the compositions are also provided.
CN1896065A 1-(3', 4', 5'-tribasic-phenyl)-isoquinoline compound, its preparation and use A 1-(3, 4, 5,-tribasic phenyl)-isoquinolyl compound, its intermediate compound or its medicinal salt or solvent, its production and use are disclosed. The compound can inhibit tumor cell activity and be used for antineoplastic.
US20060183784 Human growth hormone antagonists A method is disclosed for treating disorders in which human growth hormone is implicated by administering to a mammal an effective amount of an antagonist according to the general formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein.
WO2009058857A1 Mitigation of animal and plant diseases using bioavailable minerals A composition is able to treat plant and animal diseases and includes a therapeutically effective amount of an encapsulated ionic mineral complex and a pharmaceutically acceptable carrier. The composition may also include other inert ingredients, botanical extracts and vitamin and mineral supplements.
CN102988412A Gynecological lotion The invention discloses a gynecological lotion. The gynecological lotion comprises the following components in percentage by weight: 1-3% of sodium bicarbonate, 1.5-2.0% of metronidazole, 1.0-2.0% of benzalkonium bromide, 3-10% of propanetriol and the balance of water. The cure rate of the gynecological lotion disclosed by the invention against fungal vaginitis achieves 95%. The gynecological lotion also has the efficacy in different degrees against other gynecological diseases, such as trichomonal vaginitis, cervical erosion and the like.
EP2489663A1 Compounds as syk kinase inhibitors The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by inhibition of Syk kinase.
WO2007015569A1 Method for prediction of the efficacy of vascularization inhibitor Disclosed is a method for the prediction of the efficacy of a vascularization inhibitor. In the method, the anti-tumor effect of a vascularization inhibitor can be predicted by measuring the number of blood vessels surrounded by pericytes in a tumor and using the measurement value as a measure for the anti-tumor effect.
WO2010013640A1 Potentiator of therapeutic efficacy on infectious disease Disclosed is a therapeutic efficacy potentiator which can be used in the treatment of an infectious disease induced by a bacterium that produces a metal ion-containing peptidase, wherein the therapeutic efficacy potentiator comprises an edetic acid salt. Specifically disclosed is a therapeutic efficacy potentiator which can be used in the treatment of an infectious disease induced by a bacterium that produces a metal ion-containing peptidase, wherein the therapeutic efficacy potentiator comprises an edetic acid compound selected from the group consisting of edetic acid, an edetic acid salt and hydrates thereof.
CN1883705A Application of cysteamine and derivative thereof in preparation of medicament for improving bird flu antibody potency Disclosed is an applocation of cysteamine and a derivant thereof in preparation of medicament for improving avian influenza vaccine antibody potency, comprising feeding animals with cysteamine and the derivant thereof as feed addictive or with final feed prepared from cysteamine and the derivant thereof and basic feed; or preparing an injection of cysteamine and the derivant thereof, enjecting them into animal bodies directly or as ejection adjuvant after emulsified with mineral oil, and injecting beforehand or at the same time of vaccine injection. The invention is provided with convenience of use, ease for quantity control, and security for use.
US20120122937 Methods for inhibiting cancer cell proliferation and inducing cancer cell apoptosis Methods and pharmaceutical compositions for treating cancer utilizing compounds characterized by the following structure: and their pharmaceutically acceptable salts.
CA2574997A1 Pharmaceutical composition comprising drospirenone and ethynylestradiol A pharmaceutical composition that comprises drospirenone and ethynylestradiol with an improved dissolution rate. A method of preparation of a pharmaceutical formulation that comprises drospirenone and ethynylestradiol in order to improve its dissolution profile. Said formulation can be used to produce an anovulatory effect when administered correctly in humans.
US8426431 Substituted 2-aminoacetamides and the use thereof The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
US20080167314 Condensed Imidazole Compound And Use Thereof The present invention relates to a compound represented by the formula [I] wherein X1, X2 and X3 are each an optionally substituted CH or a nitrogen atom, and any one of X1, X2 and X3 is a nitrogen atom, X4 is an optionally substituted CH, R1 is an optionally substituted phenyl group or an optionally substituted heterocyclic group, and R2 is an optionally substituted pyridin-4-yl group, an optionally substituted pyridine-N-oxide-4-yl group or an optionally substituted pyrimidin-4-yl group, or a salt thereof. The compound has superior p38 MAP kinase inhibitory activity and MMP-13 production inhibitory activity, and is useful as an agent for the prophylaxis or treatment and the like of an inflammatory disease, an autoimmune disease, a debilitating disease, an osteoarticular degenerative disease, a neurodegenerative disease, a vascular disease, a neoplastic disease or an infectious disease.
US20110319371 Pharmaceutical formulations comprising 4-hexyl)amino]-1-hydroxyethyl}-2-(hydroxymethyl)phenol Novel pharmaceutical formulations of a beta-2 agonist for inhaled administration via the nose or mouth, and methods of using them are provided.
CN1579401A Cought and asthma relieaving preparation and its preparation method The invention is a dioxythein double effect tablet, its character lies in: the tablet is made up of two layers, one is quick release part, which can be released quickly in vivo, and it can be absorbed by human body and acts its effect of codein and asthma relieving; another layer is slow release part, which is released slowly, and maintains the blood medicine density of dioxythein in body in a long period. The product has long effect and quick effect, which can be controlled by releasing rate, its releasing rates are 38-55%, 55-85%, and above 85% in 0.5, 3 and 6 hours. The components of the quick releasing part are: dihydroxy-thein, starch, low replaced hydroxypropyl cellulose, hydroxymethyl starch sodium and magnesium stearic acid or talcum powder; the components of the slow release part are dihydroxy-thein, hydroxide cellulose, ethyl cellulose, stearic acid and magnesium stearic acid or talcum powder, which are compressed into double-layer tablet with double-layer compressor.
US20060058267 Pharmaceutical compositions comprising a NOS inhibitor This invention relates to methods of treating neurodegenerative diseases and inhibiting neurological damage, comprising administering to a patient in need of such treatment an N-NOS inhibitor in combination with a GABA-A receptor modulator.
US7109222 Thiazole or oxazole derivatives such as 5-(4-Methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethylsulfanyl)-indan-2-carboxylic acid; Hypercholesterolemia, hyperlipidemia, and diabetes This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing hyperlipidemia and hypercholesteremia in a mammal. The present invention also discloses method for making the disclosed compounds.
EP2604609A1 Aildenafil citrate crystal form o, preparation method and use thereof The invention provides a 1-[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d] pyridine-5-group)-4-ethoxy-benzenesulfonyl]-cis-3,5-dimethylpiperazine citrate or an Aildenafil citrate crystal form O and a preparation method thereof. And the invention also provides pharmaceutical compositions containing the Aildenafil citrate crystal form O and the use thereof in preparing drugs for treating Male Erectile Dysfunction (ED). The above crystal form O can be prepared through the steps of: dissolving a raw material, namely, the Aildenafil citrate in a mixture of distilled water and tetrahydrofuran, stirring, heating, filtering, stirring a filtrate, cooling, insulating heat, crystallizing, filtering and the like. The crystal form O can be adopted to prepare drugs with pharmaceutically acceptable excipients, so as to treat the male sexual dysfunction diseases.
US20060030557 Substituted pyridines having antiangiogenic activity Compounds having the formula are angiogenesis inhibitors. Also disclosed are compositions containing the compounds, methods of making the compounds, and methods of treatment using the compounds.
EP1925665A1 Use of non-viral active agents manufactured with a molecular-biological method for treating acne Using a non-viral active agent (I), prepared by molecular biological methods, for treatment of acne and acneform skin disorders, including rosacea, is new. Use of a non-viral active agent (I), prepared by molecular biological methods, for treatment of acne and acneform skin disorders, including rosacea. (I) is an antisense oligonucleotide (ASON); (stabilized) ribozyme; (mirror) aptamer; chimeric RNA/DNA oligonucleotide; naked plasmid DNA or DNA encapsulated in a liposome, especially an ASON specific for a gene that encodes a steroid hormone receptor or steroid hormone metabolizing enzyme, particularly the androgen receptor and/or 5alpha -reductase. - ACTIVITY : Dermatological; Antiseborrheic. - MECHANISM OF ACTION : Antisense inhibition of the androgen receptor and/or 5alpha -reductase gene, and therefore androgen-induced stimulation of sebaceous gland activity. When S295 immortalized human sebocytes were treated with 0.1 MicroM testosterone (T) their proliferation was significanly stimulated. When the cells were incubated for 4 hours with 1 MicroM of the oligonucleotide (S2) directed against the transcription start site of the androgen receptor gene before treatment with T, the stimulatory effect was abolished; the absorbance in an immunoblotting assay for receptor expression was then about 0.6 compared with about 1.2 for cells not treated with T. The oligonucleotide was toxic for the cells.
US20080299118 FXR Agonists for the Treatment of Malignancies Provided are certain methods of treating maligancies with farnesoid X receptor agonists. Also provided are certain methods of inducing RECK gene expression with farnesoid X receptor agonists and methods of reducing at least one feature of a cell with farnesoid X receptor agonists
EP2585109A2 Compositions and methods for preventing and treating organ injury and/or dysfunction The present embodiments relate to compositions and methods for treating the inflammatory response in a tissue or organ, such as the liver, by contacting the tissue with a tissue-specific gap junction inhibitor; and compositions and methods of reducing the toxicity of an agent by administering a gap junction inhibitor either simultaneously or sequentially with exposure to the agent. For example, inhibition of the liver-specific gap junction connexin 32 by 2 aminoethyoxydiphenyl-borate, effectively treats and/or prevents hepatotoxicity.
WO2013038308A1 SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS AS mPGES-1 INHIBITORS The present invention relates to bicyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)
US7388023 Amino acids with affinity for the α2δ-protein Certain β-amino acids that bind to the alpha-2-delta (α2δ) subunit of a calcium channel are disclosed. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders. Also disclosed are methods of making the β-amino acids.
US20110231942 Tiki1 and tiki2, wnt inhibitors This invention relates to Tiki1 and Tiki2 proteins and nucleic acids, cells expressing the same, and methods for identifying compounds that modulate Tiki1/2 activity for use in the treatment of osteoporosis or cellular proliferative disorders.
EP1660460B1 Quinoxaline derivatives as neutrophil elastase inhibitors and their use There are provided novel compounds of formula (I) wherein R1, R4, R5, G1, G2, L and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.
CN101092375B Compound of amide diketone acid, preparation method and application This invention relates to a method for preparing amide diketonic acids and their pharmaceutical application. The general structure of amide diketonic acids is shown in formula 1, wherein, R' is one or two of H, F, Cl, Br, methyl, methoxy and hydroxyl; R1 is one of H, F, Cl, methyl, methoxy and hydroxyl; R1 is one of H, F, Cl, methyl, methoxy and hydroxyl; R2 is one of H, F, Cl, Br, methyl, methoxy and nitro; R3 is one of H, methoxy and hydroxyl; R4 is one of H, F, Cl, Br, methyl, methoxy and nitro; R5 is one of H, F, Cl, methyl, methoxy and hydroxyl. The method comprises: reacting carboxylic acids and thionyl chloride to synthesize acyl chlorides, reacting with m-aminoacetophenone to obtain N-(3-acetylphenyl)-amide compounds, reacting with diethyl oxalate in the presence of sodium methoxide, and hydrolyzing to obtain amide diketonic acid compounds. The amide diketonic acid compounds can be used to prepare antiviral drugs, especially anti-AIDS drugs.
EP1551406A1 Use of indolyl derivatives for the manufacture of a medicament for the treatment of allergic rhinitis A method to treat allergic rhinitis is disclosed in which patients are administered certain indolyl compounds.
US20130065951 Compositions and methods related to mirna modulation of neovascularization or angiogenesis The present invention concerns methods and compositions for diagnosing and/or treating vascular diseases including cancer, cardiac diseases, vascular diseases of the eye, and inflammatory diseases. The methods involve measuring the levels of one or multiple miRNAs in patient samples and using the test results to diagnose and/or predict an optimal treatment regimen for the patient. Compositions described in the invention include nucleic acids that function as miRNAs or miRNA inhibitors that can be introduced to a patient to reduce or increase vascularization as needed.
WO2005030260A8 Bispecific oligonucleotide for the treatment of cns malignancies Pharmaceutical compositions for treatment of CNS malignancies comprising a sequence of bases that is complementary to portions of both the gene encoding IGFBP-2 and the gene encoding IGFBP-5 are provided. Methods of using the pharmaceutical composition in the treatment of CNS malignancy via various modes of administration are also provided.
US20100166839 Non peptidic renin inhibitors nitroderivatives Non-peptidic renin inhibitors nitroderivatives of general formula (I): A1-(Xa—ONO2)j (I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.
CN102627683A Triterpenoid saponin compounds with antitumor effects The invention discloses an application of triterpenoid saponin compounds in treating diseases relevant to tumors. The structural formula of the compounds is represented by formula (I); and in the formula (I), R<1> to R<3> are defined in the specification. The triterpenoid saponin compounds are obtained through a preparation technology comprising extraction, alkaline hydrolysis, macroporous resin refining and the like of plants of Valerianaceae Patrinia scabiosaefolia Fisch and the like. Parts of the compounds of the invention have substantial inhibition effects on eleven human tumor cell strains of A549 human non-small cell lung cancer cells, SMMC-7721 human liver cancer cells, SGC-7901 human gastric gland cancer cells and the like, and have broad spectrum antitumor effects, so the compounds can be used for treating malignant tumors as medicines or medicinal compositions.
US7815921 Using patient's leukocyte concentration after incubation with colony stimulation factor as evaluative tool in predicting susceptibility to infection, bone marrow and autoimmune diseases after chemotherapeutic treatments The present invention relates to a method for determining the hematopoietic cytocapacity of a subject comprising the steps of: (a) determining the amount of leukocytes present in a blood sample obtained from a subject, wherein said subject has been subjected to administration of a single dose of G-CSF and has been maintained for a time sufficient to allow mobilization or release of the leukocytes from hematopoietic production and storage tissues and sites of margination into the blood; and (b) determining the hematopoietic cytocapacity by assessing the amount of leukocytes determined in step (a) with the amount of leukocytes which have been mobilized or released in a control subject wherein said control subject is selected from the group consisting of subjects having (i) a high risk for a disease, disorder or complication associated with high-dose cytotoxic chemotherapy and/or hematopoietic cell transplantation, (ii) an intermediate risk for a disease, disorder or complication associated with high-dose cytotoxic chemotherapy and/or hematopoietic cell transplantation or (iii) a low risk for a disease, disorder or complication associated with high-dose cytotoxic chemotherapy and/or hematopoietic cell transplantation.
US20080114007 8-indan-5-yl-5-oxo-2-(3-piperazin-1-yl-phenylamino)-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid isopropylamide; antiinflammatory, anticarcinogenic agent, cardiovascular disease; glomerulonephritis, immune nephritis, rheumatoid arthritis, asthma, pancreatitis, HIV infection, psoriasis The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a salt, stereoisomer, tautomer, crystalline, polymorph, amorphous, solvate, hydrate, ester, prodrug or metabolite form thereof, wherein A, Y, Z, R101 and R200 are described in the specification.
WO2006029018A3 Combinatorial chemotherapy treatment using na+/k+-atpase inhibitors The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach to alleviate or eliminate certain negative effects associated with the use of certain cancer treatment agents (e.g. chemotherapy therapeutics, etc.) or regimens (e.g. radio therapies, etc.) including stimulation of the hypoxic stress response in tumor cells.
CN102964400A Preparation method and applications of dehydro-lincomycin-free lincomycin hydrochloride The invention relates to a preparation method and applications of dehydro-lincomycin-free lincomycin hydrochloride, which belong to the field of medical technologies. The preparation method disclosed by the invention comprises the following steps: dissolving dehydro-lincomycin-containing lincomycin hydrochloride serving as a raw material into water or an aqueous alcohol solution; adding palladium on carbon accounting for 1/10-1/200 of the amount of the raw material, and simultaneously stirring and introducing hydrogen into the obtained mixture to react for 1-48 hours, so that dehydro-lincomycin is all reacted to generate lincomycin; and crystallizing lincomycin. According to the preparation method, dehydro-lincomycin in lincomycin hydrochloride has a chemical reaction to generate lincomycin hydrochloride, so that dehydro-lincomycin in the raw material is completely removed; and the raw material can be used for preparing a dehydro-lincomycin-free lincomycin hydrochloride preparation, reducing the impurities in pharmaceutical products, and improving the quality of pharmaceutical products.
CN102603675A Piperazine compound and application thereof The invention discloses a piperazine compound and application of the piperazine compound served as a calcium channel blocker or/and an acetyl cholinesterase inhibitor.
WO2008027483A1 Benzofuran derivatives as modulators of the 5-ht2a receptor The present invention relates to benzofuran derivatives of the following formula (I) which are modulators of the serotonin 5-HT2A receptor and are useful in the treatment of various diseases and disorders related to the 5-HT2A receptor.
WO2005102314A1 The use of butylphthalide homologues in preparing the drug of preventing and treating cerebral ischemic The invention disclosed the use of butylphthalide homologues in preparing the drug of preventing and treating cerebral ischemic and dementia resisting thrombus and thrombocyte agglutination. The butylphthalide homologues relate to the invention are 3-(3'-hydroxyl)butylphthalide and 3-hydroxyl-3-butylphthalide.
CN101314011A Digestion promoting defecation tablet The invention relates to a stomachic and laxative tablet. The preparation method for the stomachic and laxative tablet comprises the following steps that: Chinese angelica, rhubarb, semen coicis, malts, phyllanthus emblica and so on are concentrated into heavy paste and then cooled into extract; the extract is dried, powdered and uniformly mixed with sodium bicarbonate, starch and magnesium stearate; and the stomachic and laxative tablet is obtained after granulation, drying, tablet forming, sterilization and package.
US20090036494 Administration of Pharmaceuticals A new administration regimen giving an extended plasma concentration profile of a H+, K+-ATPase inhibitor. The extended plasma profile is received by two or more consecutive administrations of a unit dose of a H+, K+-ATPase with 0.5-4 hours interval or by a pharmaceutical composition with extended release, which may be administered once daily.
CN102940602A Essence powder for body care The invention relates to a beauty health-care product, and in particular relates to essence powder for body care with beauty and health-care functions. The essence powder comprises the following components in percentage by weight: 35-50 percent of collagen, 15-20 percent of fruit fibers, 0.2-0.5 percent of polypeptide, 0.2-0.5 percent of vitamin C, 0.1-0.3 of vitamin E, 1-3 percent of honey, 2-5 percent of milk powder, and the balance of grapefruit powder. The essence powder for body care can expel toxin, reduce fat and lose weight, particularly has an excellent effect on beauty, can effectively renovate damaged skin and recover health and moisture of the skin, and avoids the aging phenomenon of drying, wrinkles, relaxation, inelasticity and the like.
EP2662090A1 Modified hyaluronidases and uses in treating hyaluronan-associated diseases and conditions Provided are combinations, compositions and kits containing a hyaluronan degrading enzyme, such as a soluble hyaluronidase, for treatment of hyaluronan-associated conditions, diseases and disorders. In one example, the products include an additional agent or treatment. Such products can be used in methods for administering the products to treat the hyaluronan-associated diseases and conditions, for example, hyaluronan-associated cancers, for example, hyaluronan-rich tumors. The methods include administration of the hyaluronan degrading enzyme composition alone or in combination with other treatments. Also provided are methods and compositions for providing sustained treatment effects in hyaluronan-associated diseases and conditions.
CN1876057A Externally applied ointment for treating mammary glands hyperplasia The invention discloses an external-use plaster for treating mammary gland hyperplasia, which is prepared from the following constituents (by weight ratio): Chinese angelica root 40-60 parts, safflower 30-50 parts, root of red rooted saliva 60-90 parts, dried body of ground beetle 50-100 parts, dried rehmannia root 100-150 parts, banksia rose 60-80 parts, leech 30-50 parts, pangolin scales 50-60 parts, wasp's nest 100-300 parts, Chinese honey locust 50-100 parts, centipede 50-100 parts, sesame oil 5000 parts.
US20080176870 Heterobicyclic metalloprotease inhibitors The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.
EP2003202A2 G protein-coupled receptor up-regulated in prostate cancer and uses thereof A novel gene (designated PHOR-1) that is highly over-expressed in prostate and other cancers and its encoded protein are described. PHOR-1 is a G protein-coupled receptor with homology to receptors involved in olfaction. PHOR-1 in normal human tissues is restricted to prostate, and this gene is highly over-expressed in prostate cancer as well as in cancers of the kidney, uterus, cervix, stomach and rectum. Consequently, PHOR-1 provides a diagnostic and/or therapeutic target for prostate cancer.
US20070275962 Heterobicyclic Compounds as Pharmaceutically Active Agents Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.
US20100004286 Novel isoindolinone derivatives having inhibitory activity against t-type calcium channel and method for preparation thereof Disclosed are isoindolinone derivatives, represented by Chemical Formula 1, having inhibitory activity against T-type calcium channels, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient. wherein R1˜R6 are as defined in the specification.
US20120301457 LIPID COFACTORS FOR FACILITATING PROPOGATION OF PRPsc The present invention embraces methods and kits for facilitating the propogation of PrPSc, and use of the same in increasing the sensitivity diagnostic assays and in identifying compounds that modulate the conversion of PrPc to PrPSc.
EP2593433A2 N-sulfonylbenzamides as inhibitors of voltage-gated sodium channels The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I): (I) or a pharmaceutically acceptable salt thereof, wherein Z, R 1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
EP1911761A1 Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions and the use thereof Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacololgical tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation.
WO2013054337A9 Extended release pharmaceutical compositions of fesoterodine A stable extended release. pharmaceutical composition is disclosed. The composition comprises particles of fesoterodine or salts thereof, one or more rate controlling polymers and one or more pharmaceutically acceptable excipients, wherein at least 90% of the total amount of particles of fesoterodine or salts thereof by volume (D90) are having size greater than about 200 microns.
CN101439029A Method for preparing micro-encapsulated astaxanthin using pure glue gum as wall material The invention relates to a preparation method of microencapsulated astaxanthin which takes pure gum as wall material, belonging to the technical field of function food additive. Astaxanthin is a naturalpigment with good physiological function but is greatly limited in use due to self solubility and instability. The method prepares the microencapsulated astaxanthin by preparing astaxanthin emulsion, homogenizing the emulsion and spray drying; at a high temperature ranging from 160 DEG C to 200 DEG C, the astaxanthin is dissolved in soybean oil in terms of 3 percent; the mixed solution, together with a wall material solution taking the pure gum as the main material, is homogenized at a pressure of 40MPa so as to obtain the stable emulsion; and then spray drying is carried out at an inlet temperature of 190 DEG C and an outlet temperature of 90 DEG C so that water-soluble microcapsules with good shapes can be obtained. The water solubility and the stability of the microencapsulated astaxanthin are improved so that the astaxanthin can be better applied in food industry, feedstuff industry and other industries.
CN102319423A Health care product for treating habitual constipation caused by internal heat due to yin deficiency The invention relates to a health care product for treating habitual constipation caused by internal heat due to yin deficiency. The health care product comprises the following raw materials in parts by weight: 20 to 60 parts of largehead atractylodes rhizome, 10 to 40 parts of stir-fried chicken gizzard membrane with vinegar, 20 to 40 parts of collagen, 10 to 20 parts of propolis, 1 to 2 parts of lycium barbarum polysaccharides, 1 to 2 parts of astragalus polysaccharides, 1-2 parts of eucommia bark polysaccharides, 1 to 2 parts of peppermint oil, 1 to 2 parts of vitamin E and an appropriate amount of refined honey. By adopting a supplement method rather than a simple reducing method, the cause of disease is eliminated, and gastrointestinal motility and bowel movement are restored.
CN102702121A New compound m-hydroxyphenyl tetrazine dicarbonamide, preparation and application thereof The invention discloses a new compound, N1,N4-di(3-hydroxyphenyl)-3,6-dimethyl-1,2,4,5-tetrazine-1,4-dicarbonamide shown in formula (I), and preparation and application thereof. The preparation of the compound comprises the steps of using 3,6-dimethyl-1,6-dihydro-1,2,4,5-tetrazine and bis(trichloromethyl) carbonate as raw materials to react with m-hydroxyaniline in an organic solvent in the presence of alkaline catalyst. The compound provided by the invention is applied for preparing medicines for treatment and prevention of human gastric cancer, ovarian cancer, liver cancer, breast cancer or lung cancer. According to the invention, the compound is rational in design, easy in operation, low in production cost and easy to obtain raw materials, and is suitable for industrialized application, and a new choice for screening anti-tumor medicines is provided.
WO2011055708A1 Isopropyl methyl phenol-containing liquid composition for oral cavity Disclosed is a liquid composition for the oral cavity which contains isopropyl methyl phenol. The isopropyl methyl phenol-containing liquid composition for the oral cavity is contains (A) a nonionic surfactant, (B) a wetting agent selected from among glycerin, propylene glycol, polyethylene glycols and sorbitol, (C) 1-menthol, (D) a para-hydroxybenzoate and (E) a fragrance material selected from among 3-octanol, 3-octyl acetate, 3-octanone and fenchone. The total amount of component (B) contained in the composition is 5-20% by mass of the total mass of the composition, and substantially no ethanol is contained in the composition. The composition exhibits high penetration and high bactericidal effect on periodontal disease-causing biofilms, is free from the unpleasant taste caused by isopropyl methyl phenol, and has excellent feeling of use and good appearance stability.
CN103432104A Transdermal patch containing pramipexole The invention discloses a transdermal patch containing pramipexole. The transdermal patch comprises a medicine carrying pressure-sensitive adhesive layer, the pramipexole, solvent and penetration enhancer, wherein the medicine carrying pressure-sensitive adhesive layer comprises acrylate pressure-sensitive adhesive containing carboxyl base groups and acrylate pressure-sensitive adhesive containing hydroxyl base groups, which form mixed pressure-sensitive adhesive; the pramipexole is dissolved in the acrylate mixed pressure-sensitive adhesive, with the content being 10 to 30 weight percent; the content of the mixed pressure-sensitive adhesive is 50 to 80 weight percent; the content of the solvent is 5 to 20 weight percent; the content of the penetration enhancer is 2 to 15 weight percent. The pramipexole can be dissolved in a mixed pressure-sensitive adhesive patch in a high concentration way and is not crystallized, the medicine availability is high, the pramipexole has good stability in pressure-sensitive adhesive matrix, and can be continuously administrated for 5 to 7 days in a transdermal way at a relatively stable permeation rate of being larger than 5.0 micrograms/cm2/h, and the application area of a pramipexole patch is smaller than 40cm2.
CN102018699A Application of Xyloketal B in preparing antiatherosclerotic medicaments The invention discloses application of Xyloketal B in preparing antiatherosclerotic medicaments. Experiments prove that: Xyloketal B has the effects of reducing the plaque area and regulating blood fat on atherosclerotic lesions, and can prevent and treat atherosclerosis by protecting vascular endothelium, regulating the blood fat level such as reducing low-density lipoprotein cholesterol (LDL-C) and raising the LDL-C, resisting oxidative stress in vivo and other action mechanisms. A novel application field of the Xyloketal B is developed when the Xyloketal B is applied to preparing the antiatherosclerotic medicaments, and the Xyloketal B is safe and non-toxic and has strong pharmacological action and good medicinal prospect.
US20110082206 Heteroatom containing substituted fatty acids Activated fatty acids, pharmaceutical compositions including activated fatty acids, methods for using activated fatty acids to treat a variety of diseases, and methods for preparing activated fatty acids are provided herein.
EP1968592B1 Formulations comprising jorumycin-, renieramycin-, safracin- or saframycin-related compounds and a disaccharide for treating proliferative diseases Jorumycin, renieramycin, safracin and saframycin related compounds formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided.
CN103275051A 7,4',5'-trihydroxyflavanone derivative and its application in preparation of liver cancer treatment medicines The invention discloses a 7,4',5'-trihydroxyflavanone derivative and its application in the preparation of liver cancer treatment medicines. The 7,4',5'-trihydroxyflavanone derivative can be used as the compound of antitumor medicines, and has a specific curative effect on cancers, especially the liver cancer. The structure of the derivative is represented by general formula (I) shown in the specification. In-vitro pharmacological experiments show that the 7,4',5'-trihydroxyflavanone derivative having the structural general formula I has an obvious antitumor activity and a good antitumor medicine exploitation and application prospect as an antitumor medicine.
EP1940788A1 1-benzylindole-2-carboxamide derivatives The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide derivatives and to their use in therapy, particulary for the treatment of obesity or nicotine dependence.
EP2167506A2 Method for producing n-methylnaltrexone bromide The invention relates to a method for producing n-methylnaltrexone bromide, a compound of the general formula (I), X' meaning an anion that is different from bromide anion, and R meaning hydrogen or a leaving group, being dissolved or dispersed in a suitable polar solvent, said solution or dispersion being mixed with a compound containing bromide anions, and the resulting reaction mixture being stirred until the n-methylnaltrexone bromide is formed and crystallized, wherein, in the case that R means a leaving group, said group is removed during or after the reaction.
US20100143404 Thiophene derivatives for up-regulating HLA-DM activity Compounds of formula (I), compositions, methods and kits are provided. The compounds and compositions may be particularly useful for modulating immunological responses. Formula (I) wherein, R1 is alkyl, aryl, or heterocyclyl; R2 is H, alkyl, aryl, heterocyclyl, OR3 or N(R3)2, R3 is H, alkyl, aryl, or heterocyclyl; R4 is H, CN, halogen, CF3, CO2R3, or C(O)N(R3)2; X is S, SO2, O, or NR3; and Y is S, O, or NR3.
CN101744827A Medicinal composition for killing chicken colibacillosis and preparation method and use thereof The invention relates to a medicinal composition for killing chicken colibacillosis, a preparation method and a use thereof, wherein the medicinal composition is prepared from the following components according to percentages by weight: 5-20% of amoxicillin, 2-3% of clavulanic acid, 6-10% of cefixime, 8-12% of fosfomycin, and accessories with left quantity. The invention is featured with scientific formulation, strong sterilization ability, low cost and convenient use; further, the medicinal composition can be directly added to animal feed or drinking water without toxic nor side effect nor medicinal residue; thus, the medicinal composition for killing chicken colibacillosis meets the standard of safe veterinary drug and ensures the safety of animal-derived food.
CN101385723A Association between an anti-atherothrombotic and an angiotensin conversion enzyme inhibitor The present invention relates to the association of an anti-atherothrombotic and an angiotensin-converting enzyme inhibitor (ACEI), and also to pharmaceutical compositions containing them, and to methods of treating vascular complications associated with diabetes, with atherothrombotic diseases, with hyperlipidaemia, with hypertension, with chronic venous diseases, with inflammation, with metabolic syndrome associated with obesity, or with cancer, with such association.
EP2059521A1 Pyrazolo[1,5-a]pyrimidines, processes, uses and compositions The invention provides novel pyrazolo[1,5-a]pyrimidines which are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation.
WO2012004330A1 Nos-inhibitor l-nil for use in chronic pulmonary diseases The invention relates to the use of NOS inhibitors, such as L-NIL, for producing an agent for treating and/or preventing chronic pulmonary diseases in humans.
CN101904857A Pressurized spray used for treating nasitis The invention provides a pressurized spray used for treating nasitis and a preparation method thereof. The appearance of the pressurized spray is a yellowish suspension, and active constituents thereof comprises eudoephedrine hydrochloride, budesonide and gentamycin sulfate as well as suspending agent, pH conditioning agent, preservative, osmotic pressure conditioning agent and the like; and distilled water serves as solvent. Compared with the prior art, the preparation has the advantages of high curative effect, little toxic and side effect, convenient administration for patients, reduced administration frequency and the like, and can be used for treating various nasitis.
US20110318382 Immunomodulatory agents and methods of use An antisense oligonucleotide compound, composition, vaccine and methods for treating a variety of conditions characterized by up-regulation of IL-10 in a mammalian subject are disclosed. The compound (i) is composed of morpholino subunits and phosphorus-containing intersubunit linkages joining a morpholino nitrogen of one subunit to a 5′ exocyclic carbon of an adjacent subunit, (ii) is capable of uptake by monocytes, lymphocytes, and dendritic cells in a mammalian subject, (iii) contains between 10-40 nucleotide bases, and (iv) has a base sequence effective to hybridize to at least 12 contiguous bases of a target sequence contained in an exon-2 or exon-4 slice site region of human IL-10 pre-mRNA.
CN101565429A Inhibitors of dipeptidylpeptidase iv The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
US7858820 Easy to process and are highly stable on storage; nutraceuticals; dietetics; anions of inner salts contribute to therapeutic and nutritional value of compound; human and animal food/feed supplement; dosage Described herein are both non-hygroscopic salts of L-carnitine and alkanoyl L-carnitine with taurine chloride (2-aminoethane-sulphonic chloride) and non-hygroscopic salts of L-carnitine and alkanoyl L-carnitine with glycine chloride which lend themselves favorably to the preparation of solid compositions suitable for oral administration. Also described are solid compositions containing said salts.
WO2013092444A1 Diazaindole inhibitors of crac Disclosed are compounds of Formula (I): Formula (I), useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.
WO2011005929A1 Piperidine derivative and its use for the treatment of diabets and obesity The present invention relates to the GPR119 agonist, N-(2-fluoro-4-(methylsulfonyl)phenyl)-5-methyl-6-(1-(5-methylpyrazin-2-yl)piperidin-4-yloxy)pyrimidin-4-amine (Compound 1, Formula (I)), and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful in the treatment of GPR119-related disorders, such as, metabolic-related disorders and complications thereof, such as, diabetes and obesity.
CN102631336A Freeze-drying orally disintegrating tablet with vitamin K1 composition for infants and preparation method for freeze-drying orally disintegrating tablet A freeze-drying orally disintegrating tablet with vitamin K1 composition for infants and a preparation method for the freeze-drying orally disintegrating tablet relate to the technical field of medicines and preparation methods for the medicines. The vitamin K1 composition for infants consists of following components including, by weight, from 11 to 20% of vitamin K1, from 20 to 33% of mannitol, from 2 to 4% of gelatin, from 56 to 60% of medium-substitution-degree hydroxypropyl-beta-cyclodextrin and from 0.1 to 0.2% of sucralose. The components of the freeze-drying orally disintegrating tablet are simple, the freeze-drying orally disintegrating tablet does not need water and does not need to be mulled over when orally taken, and disintegrating time of the freeze-drying orally disintegrating tablet in the oral cavity of a human body does not exceed 2 seconds. The freeze-drying orally disintegrating tablet is fast in absorption, high in bioavailability, few in intestinal residue, and low in side effects and liver first-pass effect, tastes good, and is particularly suitable to be taken by infant patients.
EP2035377A1 Indole derivatives and their use as thyroid receptor ligands The invention provides compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, (I) wherein R1, R2, R3, R4, R5, R6, Y and W are as defined in the specification. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition that may be treated with a thyroid receptor agonist or partial agonist.
EP1671650A1 Combinations of nicotinic acid and derivatives thereof and sterol absorption inhibitor(s) and treatments for vascular indications The present invention provides compositions, therapeutic combinations and methods including: (a) at least one of nicotinic acid or derivatives thereof; and (b) at least one substituted azetidinone or substituted b-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.
US20080176952 Management of Ophthalmologic Disorders, Including Macular Degeneration A drug may be used in the preparation of a medicament for the treatment or prevention of an ophthalmologic disorder, wherein the drug inhibits, antagonizes, or short circuits the visual cycle at a step of the visual cycle that occurs outside a disc of a rod photoreceptor cell.
CN101259265A Deep-sea fish collagen oral liquid An abyssal fish collagen oral liquid relates to a collagen oral liquid. The present invention solves the problem that the present collagen oral liquid is not capable of supplying water to skin. The abyssal fish collagen oral liquid of the present invention mainly consists of abyssal fish collagen, chitine extract, orange juice, grapefruit juice, apple juice, spice, granulated sugar, fructose syrup, citric acid, lactic acid, sodium citrate, vitamin E and water. The acid mucopolysaccharide formed in human body by the product of the present invention can supply water directly and moisten the skin, and at the same time can improve the microcirculation and strengthen the moistening degree of the skin, thus improving the water-retaining ability of skin, being elastic, reducing the wrinkles, taking the effect of complete skin protecting and solving the problem that skin lacks water.
CN101040846A Nonoxinol foaming agent and the method of preparing the same The invention relates to a benzene octanol foaming agent and relative preparation, characterized in that filling main materials and findings as benzene octanol into a container, screwing and covering a foaming pump (or a hand-operated foam generator), pressing the pump via hand to generate foam. And the production comprises that adding water into benzene octanol to dissolve, adding polysorbate-80, dodecyl sodium sulfate, and glycerin or the like, mixing uniformly, adding distilled water to total weight, mixing uniformly, adjusting pH value, filling into the container, screwing and covering the foaming pump (or hand-operated foam generator), pressing the pump via hand to generate foam, or adding injection agent to generate foam. The foaming agent can uniformly distribute in vagina and skin, with wide application and quick speed for penetrating into vagina mucosa, to effectively treat disease. And the benzene octanol has strong disinfection and spermaticide functions, for treating local gynaecology infection and contraceptive property.
CN101805383B Strictosidine lactam derivatives and preparation method and use thereof The invention provides novel strictosidine lactam derivatives and pharmaceutically acceptable salts thereof, which have the following general structural formula. The invention also provides a preparation method, which is characterized in that serotonin derivatives and split-ring brucine are catalyzed by immobilized strictosidine synthase and mutants to obtain the novel strictosidine derivatives, and then the strictosidine derivatives are catalyzed by base to synthesize the derivatives by one step. The in vitro cytotoxicity activity test of compounds provided by the invention shows that the derivatives inhibit the growth of tumor cells and can be applied to the preparation of drugs for preventing and controlling tumor diseases.
US20090099245 Title compound is Veliparib, a Poly(ADP-ribose) polymerase i.e. PARP inhibitor; anticancer agent 2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide Crystalline Form 1, ways to make it, compositions comprising it and made using it, and methods of treating patients having disease using it are disclosed.
CN102488709A Florfenicol-zinc chelate injection and preparation method thereof The invention discloses a florfenicol-zinc chelate injection and a preparation method thereof. The injection comprises components of, by weight: 10-50 parts of florfenicol, 1-5 parts of zinc salt, 15-65 parts of an amide solvent, and 10-65 parts of an auxiliary solvent. The preparation method of the florfenicol-zinc chelate injection comprises steps that: the amide solvent with the above weight proportion and approximately 80-95% of the auxiliary solvent are mixed with the zinc salt; the mixture is heated to a temperature of 65-75 DEG C, and the temperature is maintained for 1.5-2.5h; florfenicol is dissolved in the mixed solution; rest of the auxiliary solvent is added to the mixed solution; the solution is filtered by using a sand-core filter stick; an obtained clarified solution is encapsulated, and is subject to Arnold steam sterilizing under a temperature of 115 DEG C. The injection provided by the invention is advantaged in good syringeability, good physical stability and good chemical stability. Compared to a florfenicol injection solution that does not contain zinc, the antibiotic function of the injection provided by the invention is higher. The dosage of florfenicol can be reduced, such that the generation of bacteria drug resistance can be reduced. The injection and the method satisfy the requirements of animal-use product and food safety.
WO2007002742A1 Substituted [1,4]-diazepanes as cxcr3 antagonists and their use in the treatment of inflammatory disorders CXCR3 inhibitors of formula are disclosed. Inhibition of CXCR3 activation is useful for treating disorders resulting from CXCR3 -associated T-cell mediated function, such as inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis and diabetes, as well as in the prevention of allograft rejection. N-ethyl-l,4-diazepane-l-carboxamides in which R1 is substituted or unsubstituted arylalkyl and R3 is substituted or unsubstituted aryl are particularly preferred.
WO2010117084A1 Novel isoquinoline derivatives The present invention relates to a compound represented by a formula (I): wherein: R is independently from each other a lower alkyl group and the like, X is an oxygen atom or a sulfur atom, Y is a lower alkylene group having 1 to 6 carbon atoms, R1 is a phenyl group and the like which may be substituted by a halogen atom and the like, and any CH2 in the following: (I-1) may be substituted by a lower alkyl group, and R2 is a phenyl group or a pyridinyl group which may be substituted by a lower alkyl group and the like, m is 0, 1, 2 or 3, and n is 0 or 1, or a pharmaceutically acceptable salt thereof.
CN1814167A Health-care for diabetes The invention is a health product for diabetes, relating to the field of health products, prepared of Oyster Shell extract, Se-enriched yeast, Cr-enriched yeast, Lí¬zinc aspartate, L- magnesium aspartate, linolenic acid powder, alpha- Thioctic Acid, Bitter Melon P.E, P. tataricum Linn extract, Fructus lycii P.E, Dwarf Lilyturf Tuber extract, Cortex Mori extract, Fructus Corni extract, and Fenugreek P.E, and it can promote insulin function to be normal, synthetically supplement nutrition deficient in the diets of patients suffering from diabetes, prevent complication of diabetes, protect brain, eyes, and heart, promote cooperation of immune system, nerve system and endocrine system and synthetically regulate blood sugar to be stable.
CN101723990A Complex salt consisting of glucuronic acid or glucurolactone and kushenin or matrine and application thereof The invention relates to the medicament field, in particular to a complex salt consisting of glucuronic acid or glucurolactone and kushenin and/or matrine, a method for preparing the complex salt, application of the complex salt in treating liver diseases, in particular the diseases such as hepatitis, hepatic injury, liver cancer and the like, and a complex salt medicament capable of being used as an oral administration dosage form as well as a non-oral administration dosage form. Pharmacodynamic laboratory science for comparing the complex salt with the glucurolactone, sodium glucuronate, the kushenin and the matrine shows that the functions of the complex salt are better than that of using the glucurolactone, the sodium glucuronate, the kushenin and the matrine independently. The enhancement action is proved on a plurality of animal models.
CN102872062A Medicinal composition for treating or preventing obesity and metabolic syndromes The invention discloses a medicinal composition for treating or preventing the obesity and metabolic syndromes, and belongs to the medicine field. The medicinal composition treats orlistat and acarbose as medicinal active components, so the application amount of orlistat in the medicinal composition is substantially reduced, thereby the risk of the damage of orlistat to the liver of a body is reduced. The medicinal composition has a substantial synergistic effect when the medicinal composition is used for treating or preventing the obesity and the metabolic syndromes, can reduces the diabetes and angiocardiopathy suffering risks of obese patients, and has a wide medical application prospect.
EP1853266B1 2s,4r ketoconazole for treating diabetes, metabolic syndrome and other conditions Pharmaceuticals compositions comprising the 2S, 4R, ketoconazole enantiomer or its pharaceutically acceptable salts, hydrates, and solvates, that are substantially freee of the 2R, 4S ketoconazole enantiomer are useful to reduce cortisol synthese and for the treatment of type 2 diabetes, hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other diseases and conditions, including but not limited to Cushing's Syndrome, depression, and glaucoma.
CN100998589A Novel use of Enduotai, hard capsule thereof, and method for preparing the injection An application of Endothal (EDT or norcantharidine) in preparing capsule or injection for treating lung cancer, intestinal cancer, breast cancer, leukemia, ovary cancer, etc is disclosed. Its preparing process and content measuring method are also disclosed.
CN101161290A Beta-elemi alkene polyglycol amine derivant as well as its synthesis method and purpose A beta-elemene glycol amine derivative as formula I is disclosed in the present invention, wherein, R1, R2, solely are H or -NH(CH2CH2O)nCH3, condition is that R1 and R2 are not H at the same time, n is integer from 1 to 454; or its pharmaceutical acceptable salt. The synthesizing method of beta-elemene glycol amine derivative and its use in preparing medicine for treating cancer are also disclosed in the present invention. The beta-elemene glycol amine derivative of the present invention has better water soluble and better anti-cancer active than that of beta-elemene.
WO2012125871A2 Aconitine compounds, compositions, uses, and preparation thereof Compound derivatives of aconitine are provided, in particular derivatives that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. The subject compounds are useful in treatments, including treatments to modulate neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the aconitine derivatives.
US6878708 Imidazotriazinones and the use thereof Novel imidazotriazinones of general formula (I), a method for the production and the pharmaceutical use thereof are disclosed.
EP2182959A1 Composition and treatment Disclosed are compositions for the treatment of neuropathy and in particular peripheral neuropathy. The compounds include low molecular weight glycosaminoglycans. The peripheral neuropathy may be due to cancer treatment drugs.
US7718191 Pharmaceutical product which is used to reduced or stop moderate or severe snoring The invention relates to the novel use of a pharmaceutical product which combines domperidone and pseudoephedrine sulphate substances and which can be used to reduce or stop moderate or severe snoring.
US20120046251 Inhibitors of soluble epoxide hydrolase to inhibit or prevent niacin-induced flushing The invention discloses methods of using cis-epoxyeicosantrienoic acids (“EETs”), inhibitors of soluble epoxide hydrolase (“sEH”), or a combination of an EET and an inhibitor of sEH, to reduce or prevent niacin-induced cutaneous vasodilation (“flushing”) in subjects suffering from this undesirable side effect of receiving therapeutic amounts of niacin.
US20130059897 Rapid release irbesartan-containing pharmaceutical composition The present invention relates to an irbesartan-containing pharmaceutical composition, in particular a tablet thereof, which comprises the active ingredient, a disintegrant with at least one low-substituted hydroxypropyl cellulose.
CA2190515C Vaccine against mycobacterial infections A naked nucleic acid construct comprising a coding sequence which encodes a mycobacterial stress protein or proline-rich antigen or an antigenically effective fragment thereof operably linked to a promoter capable of expressing the said coding sequence in a mammalian host cell is useful as a vaccine against a mycobacterial infection such as tuberculosis and leprosy.
CN102579393A Solid composition for improving content uniformity and dissolution rate of imidafenacin The invention relates to a solid composition containing imidafenacin. The solid composition can improve the dissolubility and content uniformity of main medicines effectively.
WO2013178075A1 N-aryl unsaturated fused ring tertiary amine compound, preparation method thereof and antitumor application thereof An N-aryl unsaturated fused ring tertiary amine compound, a preparation method thereof, a pharmaceutical composition containing the compound, and an application thereof in preparing medicine for treating tumors.
CN1615889A Medicine for treating skin disease The medicine for treating skin disease consists of the following materials: halcinonide, menthol powder, camphor powder, dexamethasone acetate, Benadryl hydrochloride, miconazole nitrate, chloromycetin, griseofulvin, propylene glycol, sodium benzoate, sulphur powder and aromatic vanishing cream. The preparation process includes grinding and mixing menthol powder, camphor powder, dexamethasone acetate, Benadryl hydrochloride, chloromycetin and griseofulvin; mixing with sulphur powder and 100-mesh sieving; adding halcinonide, miconazole nitrate, propylene glycol and sodium benzoate while stirring; and finally adding vanishing cream. The present invention is wide spectrum antibacterial medicine and suitable for various kinds of fungi caused skin diseases, and has determined and fast curative effect, no toxic side effect and low cost.
US20080081069 Novel controlled release formulations of divalproex sodium A controlled release formulation comprising less than about 40% of anti-epileptic drug, about 20% to about 50% of rate controlling polymer and silica having a particle size less than about 1 micron and specific surface area not less than 70 m2/g, all weight percentages are based upon the total weight of the dosage form, manufactured under normal atmospheric conditions.
WO2010092467A1 Medicament comprising terpenoid cholinesterase inhibitor for treatment of dismotility disorder The present invention refers to the use of certain terpenoids having high cholinesterase inhibitory activity in the manufacturing of a composition to treat a foregut dysmotility disorder, wherein said terpenoids act as prokinetic agent by fastening the postprandial gastric empty. The composition may further comprise a gastric pH-modifier agent such as an antacid, a proton pump inhibitor, a H2-receptor antagonist, or a parietal cell activator.
CN1739538A Suppository for teating mycotic vaginitis The suppository for treating mycotic vaginitis contains tinidazole, fungicidin and chlorhexidine in certain proportion, and is prepared through mixing tinidazole, fungicidin and chlorhexidine in certain proportion in some container and filling into administration unit with each suppository weighing 0.5 g. The suppository is administrated via vagina and absorbed through mucous membrane to kill fungi in vagina. It may also promote the proliferation of epidermis cell in vagina, regulate pH value in vagina, raise antifungus capacity, improve the permeability of cell membrane and reduce exudation and has no negative effect.
CN103228656A 3-substituted-6-(pyridinylmethoxy)- pyrrolopyridine compounds The invention provides certain 3-substituted-6-(pyridinylmethoxy)-pyrrolopyridine compounds, particularly compounds of formula I and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat Parkinsons disease.
WO2010052222A1 (dihydro)naphthyridinone derivatives as histamine h3 receptor antagonists The invention relates to compounds of formula (I), wherein X1a, X2a, X1 to X5, n and R have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
CN101302199A Guidemycin and use thereof in tumor treatment The invention relates to a kueide mycin which is a novel derivative of geldanamycin. According to the anticancer activity experiment, kueide mycin has in both vitro and vivo antitumor activities. The kueide mycin has the in vitro activity characteristics of inhibiting tumor cell proliferation, inducing the tumor cell apoptosis, reducing related target proteins of Hsp 90 in the tumor cells, as well as inhibiting the tumor cell migration, and has in vivo antitumor activity characteristics of notably reducing poisonousness compared to the geldanamycin. The kueide mycin can obviously inhibit the growth of solid tumor of a nude mouse model of Human breast carcinoma xenografts after being injected in a peritoneal cavity and is expected to be developed into a clinical effective antitumor drug.
CN101607040A Drug for curing knife and gun injury and traumatic injury ulcerate as well as preparation method thereof The invention discloses a drug for curing knife and gun injury and traumatic injury ulcerate, which is prepared by the following materials by weight percent: 10-20 of ampelopsis japonica, 10-20 of angelica, 10-20 of ligusticum wallichii, 10-20 of forsythia, 10-20 of pollen typhae, 10-20 of nail tip, 10-20 of bletilla striata, 10-20 of pseudo-ginseng, 1-10 of frankincense, 1-10 of myrrh, 0.05-0.5 of borneol, 1-3 of vermilion, 0.05-0.5 of muskiness, 2-10 of daemonorops draco and 11-21 of saffron. The drug not only can cure traumatic injury, knife and gun injury and ulcerate, but also can cure sore, fistula, furuncle, and the like, but also has obvious effects. The drug for curing knife and gun injury and traumatic injury ulcerate has the effects of activating blood to resolve stagnation, relieving swelling and pain, accelerating cell and issue regeneration, expanding granulation from inside to outside, and having no infections.
EP2376478A2 Pyridyloxyindoles inhibitors of vegf-r2 and use thereof for treatment of disease The invention relates to novel organic compounds of formula (I), and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.
CN201578610U Combined capsule filled with pamabrom solid preparation and acetaminopher solid preparation The utility model relates to a combined capsule filled with pamabrom solid preparation and acetaminopher solid preparation in a capsule. The combined capsule comprises a first capsule and solid preparation in the first capsule, wherein the first capsule comprises an upper capsule body and a lower capsule body, and at least a solid preparation with acetaminopher active component and at least a solid preparation with pamabrom active component are filled in the first capsule. Compared with the prior art, the combined capsule has the following advantages that each component can not generate chemical change and accessory substances, and stability of products is improved. The combined capsule is extremely suitable for industrial production, and compliance of patients is also excellent.
EP0954317B1 Use of 7 apha-substituted steroids to treat neuropsychiatric disorders Use is provided for a 7α-hydroxy or 7-oxo substituted 3β-hydroxy-steroid possessing the carbon skeleton of cholesterol, androsterone, pregnenolone or estradiol, or an analogue thereof substituted independently at one or both of the 7- and 3-positions with an ester or ether group, in the manufacture of a pharmaceutical composition for the therapy of neuropsychiatric, immune and/or endocrine disorders or for inducing cognitive enhancement. Uses for Cyp7b enzymes in producing such steroids is also provided together with various novel steroids and test kits and methods for diagnosing the disorders.
US20050043346 Pyridylpyrrole derivatives active as kinase inhibitors Pyridylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
US20100160427 Method of treating vascular injuries induced by an excess of plasma lipids using combinations of vasoprotective agents Combinations of vasoprotective agents useful for the prevention and the treatment of vascular injuries induced by an excess of plasma lipids comprising polycosanols, tocotriends and/or lycopene, procyanidole oligomers and vegetable oil rich in insaturated fatty acids.
US7642283 modulating the activity of the mitochrondrial permeability transition pore complex comprising exposing the complex to a compound such as 6-bromo-3-methylene-chroman-4-one Methods of utilizing compounds of general formulas I and II as modulators and affinity labels of the MPTP complex are elucidated. Furthermore, methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component are identified. Moreover, novel compounds of general formulas I and II are disclosed.
CN102727444A Entecavir solid dispersion, pharmaceutical composition, method for preparing entecavir solid dispersion and pharmaceutical application of entecavir solid dispersion The invention belongs to the technical field of pharmacy, and in particular relates to an entecavir solid dispersion, a method for preparing the solid dispersion and a pharmaceutical application of the solid dispersion. The entecavir solid dispersion disclosed by the invention comprises entecavir and lactose or lactose and other additives, wherein the mass ratio of entecavir to lactose or lactose and other additives is 1: (10 to 500) or 1: (100-200): (50-90). The invention further discloses application of a pharmaceutical composition. By the process, the problems that the entecavir preparation with small specification has high content uniformity requirement on pharmaceuticals and stable properties can be effectively solved; and moreover, the entecavir solid dispersion has the characteristics of good water solubility, quick dissolution rate, no organic solvent residue, low production cost and simple process, and is specially suitable for industrial production.
US20090286833 Substituted Cyclohexylmethyl Compounds Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.
CN1579407A Nasal administration preparation for anti-AIDS-virus brain infection and use thereof The invention discloses a nasal cavity administration preparation which can resist the brain infection of aids, it belongs to medicine preparation technology field for anti-aids virus, it uses hydroxyl inosine as pharmacologic active ingredient, adds in pH value regulator, penetration advancing agent, thickener, equal-penetration regulator, antiseptic and produces them into preparation suitable for nose cavity, solves the problem that the current medicine with oral, muscle injection or other modes the medicine can penetrate the vein blood brain barrier to the brain, the release and absorption of the preparation in the invention are quick, the medicine can gathers in the brain, the medicine density in brain is upgraded prominently, at the same time, the invention has character that the nose cavity mucous coat and cilium toxin are small.
CN102357094A Pharmaceutical composition containing eighteen amino acids The invention relates to a pharmaceutical composition containing eighteen amino acids. A preparation method of the pharmaceutical composition containing eighteen amino acids comprises the following steps of feeding nitrogen gas having purity of 99.9% into a concentrating tank, pouring 750000ml of injection water into the concentrating tank, simultaneously, adding a prescription amount of sorbitol into the concentrating tank, stirring for 5 minutes until the sorbitol is dissolved fully and is mixed well, adding seventeen monomer amino acids into the mixed solution obtained by the previous step, stirring for 10 minutes until the seventeen monomer amino acids are dissolved fully, adding active carbon of which an addition amount is 0.05% of a final preparation amount into the mixture obtained by the previous step, stirring for 20 minutes, carrying out backflow for 15 minutes, cooling the concentrated solution obtained by the previous step, carrying out decarburization by a titanium bar filter until the concentrated solution is clear, filtering the clarified concentrated solution by the titanium bar filter, feeding the filtrate into a dilution tank, adding an appropriate amount of water into the dilution tank, adding NaHSO3 of which an addition amount is 0.05% of a preparation amount into the dilution tank, cooling, adding a prescription amount of tryptophan into the dilution tank, supplying injection water until the mixed solution in the dilution tank has a final prescription volume, stirring for 10 minutes, adjusting a pH value of the mixed solution in the dilution tank to a pH value of 3.8 to 4.3 by sodium hydroxide or hydrochloric acid, carrying out sampling, detecting total amino nigrogen content, tryptophan content and a pH value of the mixed solution, and adjusting the total amino nigrogen content, the tryptophan content and the pH value of the mixed solution so that the total amino nigrogen content, the tryptophan content and the pH value are in internal control ranges. The pharmaceutical composition containing eighteen amino acids overcomes the defect that adverse reactions can be produced in preparation adopting the prior art.
CN102240284A Pharmaceutical composition with fenticonazole used as active ingredient The invention relates to a pharmaceutical composition with fenticonazole used as a main ingredient. The pharmaceutical composition is a pharmaceutical preparation prepared from fenticonazole and pharmaceutically acceptable salts used as the main ingredients and appropriate types of pharmaceutical excipients. The fenticonazole pharmaceutical preparation has stable and controllable quality and is safe and effective.
US20100151005 Targeted carriers for intracellular drug delivery The invention provides a method for delivering a cargo molecule into a cell using a targeted DNA-based carrier (e.g., DNA dendrimer). Compositions and kits useful in the practice of the methods are also provided.
CN102746360A Synthesis and application of four new conjugates of camptothecin-steroid The invention discloses the synthesis and application of four new conjugates of camptothecin-steroid. The four new conjugates of camptothecin-steroid are: 1) the name of the first new conjugate is 20 (S)-O-3 beta-hydroxy-5-androstene-17 beta-acyl camptothecin, CPT-1 for short; 2) the name of the second new conjugate is 20 (S)-O-3 beta-acetoxy-5-androstene-17 beta-acyl camptothecin, CPT-2 for short; 3) the name of the third new conjugate is 20 (S)-O-androst-4-alkene-17 beta-acyl camptothecin, CPT-3 for short; 4) the name of the forth new conjugate is 20 (S)-O-4-aza-5 alpha-androst-3-ketone-17 beta-acyl camptothecin, CPT-4 for short; By employing EDCI-DMAP coupling method, all the four new conjugates of camptothecin-steroid are synthesized based on raw materials of camptothecin and four steroid acids. The compounds of the invention have good antineoplastic activity, and great prospect in pharmaceutical development.
CA2429486C O/w emulsion composition and method of preparing the same The present invention provides an O/W emulsion composition containing an adenosine phosphate or salt thereof. More particularly, the invention provides an O/W emulsion composition which has excellent emulsion stability. The O/W emulsion composition of the invention can be prepared using an adenosine phosphate or salt thereof, a polyglycerin fatty acid ester, an alkanoyl lactylic acid or the salt thereof, an acrylic acid-alkyl methacrylate copolymer, water, an oil, and preferably, a polyhydric alcohol.
US20080188425 Dihydroouabain-like factor and diagnostic & therapeutic compositions and methods A novel mammalian dihydroouabain-like factor is disclosed which substantially fails to cross-react with mammalian ouabain-like factor (OLF) for binding to anti-OLF antibody, but cross-reacts with plant-related dihydroouabain (dho) for binding to anti-dho antibody, has maximal u.v. absorbance at 196 nm, has a non-peptidic, non-lipidic chemical structure and a fully hydrogenated lactone ring, has a concentration-dependent Na+,K+-ATPase (sodium pump) catalytic inhibitory activity which is 10-fold lower than OLF and 3-fold higher than plant-related dihydroouabain, and a high pressure liquid chromatography elution time about the same as dho. This factor is useful for therapy for congestive heart failure. An antibody and antibody fragments having affinity for mammalian Dh-OLF but not for OLF, and diagnostic and therapeutic methods comprise the antibody and means for quantifying the antibody and are useful for treating a condition caused by high level of OLF or Dh-OLF. Two isomers of plant-related dihydroouabain have been isolated. These compositions and methods are suitable for characterizing a variety of diseases and conditions associated with reduced sodium pump activity.
WO2006032144A1 Pharmaceutical compositions and methods relating to inhibiting fibrous adhesions or inflammatory disease using fucans from various echinoderm sources Compositions and methods for the treatment, prevention, inhibition, etc, of inflammatory disease or fibrous adhesions involving administration of fucans from various echinoderm sources, alone or in combination with other agents useful for the treatment, prevention, inhibition, etc, of fibrous adhesions or inflammatory disease. The anti-fibrous adhesion agents provide significant therapeutic effect against fibrous adhesions while typically also providing low side effects. Further, since avariety of different anti-fibrous adhesion agents are discussed, various combinations of the agents can be selected as desired to reduce side effects in patients potentially suffering from other diseases or conditions and/or to provide other beneficial healthful or therapeutic effects, such as compositions that both inhibit fibrous adhesions and also treat cancer or arthritis or swelling or any of the variety of other diseases or conditions that can also be treated by one or more of the anti-fibrous adhesion agents herein. The compositions herein are also useful for the treatment of fibrous growths and conditions such as keloid trait that share similar biology with fibrous adhesions.
WO2004080933A3 Isolation of lutein from alfalfa The present invention provides a process for an industrial scale extraction and purification of xanthophylls ( e.g., lutein and zeaxanthin) from plant material (e.g., alfalfa or other leafy green crops having high levels of chlorophyll). The process involves harvesting lutein rich alfalfa, extracting an oleoresin from the alfalfa leaves, saponifying the oleoresin, extracting and extracting lutein using a series of solvent extractions specific for oleoresin obtained from alfalfa or other leafy green plants.
US20080021030 Substituted Pyrazoles As Ppar Agonists A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein: p is 0 or 1; q is 0 or 1; R1 and R2 are independently H or C1-3 alkyl; R3 and R4 are independently H, C1-6 alkyl, —OC1-6 alkyl, halogen, OH, C2-6 alkenyl or CF3; R5 is H, or C1-6 alkyl, wherein said C1-6 alkyl is optionally substituted by one or more halogens, —COphenyl, —OC1-6 alkyl, phenyl, morpholino, or C2-6 alkenyl; R6 is C1-6 alkyl, halogen, —OCH2 phenyl, morpholino, pyrrolidino, piperidino, thiophenyl, furanyl, pyridinyl, —OC2-6 alkenyl, or phenyl, wherein said phenyl is optionally substituted by C1-3 alkyl.
US20130058926 Method for alleviating and/or preventing skin reddening A method of alleviating and/or preventing skin reddening for a subject in need thereof by means of inhibiting angiogenesis at the site of the reddened skin, is provided.
EP1368325B1 New asymmetric process for the preparation of diarylmethylpiperazines derivatives and novel asymmetric diarylmetylamines as intermediates An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.
EP1019060B1 Androgen synthesis inhibitors This invention relates to novel inhibitors of androgen synthesis that are useful in the treatment of prostate cancer and benign prostatic hypertrophy. The present invention also provides methods of synthesizing these novel compounds, pharmaceutical compositions containing these novel compounds, and methods of treating prostate cancer and benign prostatic hypertrophy using the androgen synthesis inhibitors of the present invention.
US20060058385 Combination of antidiabetic drugs The combination of R-4-trimethylammonio-3-(tetra-decylcarbamoyl)-aminobutyrate and metformin is disclosed. Said combination of anti-diabetic drugs exerts a synergic action and allows the administration of the two drugs at doses such as to avoid or reduce the occurrence of side effects. The combination is also useful for improving the therapeutic cover far from mealtimes, and in postabsorption and fasting conditions.
EP2066648A1 Substituted dimethylcyclobutyl compounds, their preparation and use in medicaments The present invention relates to substituted dimethylcyclobutyl compounds of general formula I, a process for their preparation, medicaments comprising said substituted dimethylcyclobutyl compounds as well as the use of said substituted dimethylcyclobutyl compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via sigma receptors.
CN103751197A New use of stibene glucoside in preparing medicament for treating Alzheimer disease The invention aims to disclose new use of stibene glucoside in preparing medicament for treating Alzheimer disease. Experiments in which APP695V717I transgenic mouse is used to simulate nerve cell damage in Alzheimer disease prove that pre-administered stibene glucoside can significantly improve behavioral disorders of model mouse by improving brain blood circulation, reducing expression of apoptosis factor Fas/FasL and inhibiting excitatory amino acid level, suggesting that stibene glucoside has distinct protective effect on nerve cell damage in Alzheimer disease. Stibene glucoside prevents and treats Alzheimer disease through multi-target action, stibene glucoside and related adjuvants can be prepared into health products or medicaments for improving cognitive function and treating Alzheimer disease by conventional preparation method. The health products or medicaments can be used for delaying and improving cognitive function and slowing down the progression of Alzheimer disease, and improving physical constitution and life quality of the elderly.
CN102908334A Oxygen-contained capsule An oxygen-contained capsule is provided with a capsule skin. Oxygen is wrapped in the capsule skin, the particle size of the oxygen-contained capsule is 0.8 nanometers-8 millimeters, and the oxygen in the capsule skin is oxygen gas or an oxygen-contained solution. When the oxygen in the capsule skin is the oxygen gas, the concentration of the oxygen gas is 21-99.99%. When the oxygen in the capsule skin is the oxygen-contained solution, oxygen quantity in the oxygen-contained solution is 11-20mg/L. After the oxygen-contained capsule is taken, the oxygen-contained capsule can rapidly explode to form reactive oxygen. Oxygen molecules are strong in seepage force and high in purity, parts of the oxygen molecules can be soluble to an aqueous solution in intestinal tracts to form active high-oxygen water, and parts of the oxygen molecules can be directly absorbed by the stomach and intestine of a human body.
WO2011147198A1 Compounds and methods for treatment of proliferative diseases Cell based and cell-free assays for identifying compounds that promote aggregation of proteins, glycoproteins, and protein-nucleic acid complexes are disclosed. Also disclosed are compounds, formulations and methods for treating or preventing viral infection, bacterial infection, cancer, or diseases involving hyper-proliferative cells.
EP1467769B1 Use of a resinate in the preparation of a formulation for smoking cessation A highly productive and environmentally friendly method of loading pharmaceutically active substances onto ion exchange resins using a water miscible or water-immiscible solvent is disclosed.
EP1467622A4 Mitocidal compositions and methods Methods for the treatment and prevention of cutaneous mites and for the treatment and prevention of cutaneous inflammation of mammalian skin associated with cutaneous mite infestations utilizing compositions comprising fulfur, one or more sulfur derivative and a dermatologically acceptable carrier. The composition is preferably a cleanser.
CN101301273A Anticancer composition containing satraplatin The invention discloses an anticancer composition containing satraplatin which is a sustained release injection and a sustained release implant. The sustained release injection consists of sustained release microspheres and menstruum, wherein, the sustained release microspheres comprise effective anticancer components and sustained release excipient, and the menstruum is ordinary menstruum or special menstruum containing a suspending agent. The viscosity of the suspending agent is between 100 and 3000cp (at the temperature of between 20 and 30 DEG C) and is selected from sodium carboxymethyl cellulose and so on; the sustained release excipient is selected from organic phosphate polymers such as p (LAEG-EOP), p (DAPG-EOP) and so on, or polymers or blend of polyphosphate ester and polylactic acid, polifeprosan, decanedioic acid, PLGA and so on; the sustained release implant comprises the effective anticancer components and the sustained release excipient, the injection or the placement of the anticancer composition inside a tumor or at the tumor circumference can maintain the effective medicine concentration up to more than 60 days, can also apparently decrease the systemic reaction of the medicine, and selectively enhance the treatment effect of non-operative treatments such as chemotherapy and radiotherapy (including inner radiotherapy) and so on.
CN103006658A Application of piperazinyl-containing benzonitrile in preparing anti-fungal infection medicament The invention relates to an application of piperazinyl-containing benzonitrile in preparing an anti-fungal infection medicament, and in particular discloses a compound 3-((4-(2-aminoethyl)-piperazidine-1-yl)benzonitrile or pharmaceutically acceptable salt thereof, and a preparation method and a medical application thereof. The piperazinyl group substituted benzonitrile compounds is easy in synthesis step, simple and practical in preparation method, convenient and easily available in raw material source, low in cost and small in pollution. The compound has remarkable activity of inhibiting fungus growth, and the MIC (minimal inhibitory concentration) value of the compound is 62.5mg/ml. Pharmacodynamic results indicate that piperazinyl group substituted benzonitrile compound or pharmaceutically acceptable salt thereof can be expected to be used as a medicament for preventing and treating diseases caused by fungal infection.
WO2008046160A1 Assay for the detection of biomarkers associated with pregnancy related conditions The invention relates to screening methods for determination of the risk of preterm delivery and/or pregnancy associated conditions. The methods involve detection of the level of one or more biomarkers in a biological sample from the patient. In particular, in embodiments of the invention there are provided methods for determining the risk of pre-eclampsia and other hypertensive disorders, and intrauterine growth retardation (IGUR).
CA2524495A1 Modulation of survivin expression Compounds and compositions are provided for modulating the expression of survivin. The compounds, exemplified by those acting through an RNAi antisense mechanism of action, include double-stranded and single-stranded constructs, as well as siRNAs, canonical siRNAs, blunt-ended siRNAs and single-stranded antisense RNA compounds. Methods of using these compounds for modulation of survivin expression and for treatment of diseases associated with expression of survivin are provided.
US20080182857 Heat Shock Protein 90 inhibitors; 5-(2,4-dihydroxyphenyl)-4-(naphth-1-yl)-4H-1,2,4-triazole-3-thiol; incorrect protein folding or aggregation; hydrazonederivatives react with dimiadazole cabonyl/thiocarbonyl derivatives; hydrazines derivatives react with isocyanate or isothiocyanates; tumors, cancer Novel triazole derivatives of the formula (I), in which R1-R6 and Y have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
WO2006108666A1 Mefloquine, nelfinavir and saquinavir as novel agents for neurodegenerative and (neuro-) inflammatory diseases The present invention generally relates to the neuroprotective, anti-apoptotic and anti-inflammatory activity of mefloquine, nelfinavir and saquinavir and derivatives thereof based on recently discovered interactions with prohibitin and estrogen receptors and the inhibition of mitochondrial voltage- dependent anion channel 1. Thus, mefloquine, nelfinavir and saquinavir and derivatives thereof may be used as medicaments for the prevention and/or treatment of neurodegenerative and inflammatory, particularly neuroinflammatory diseases.
CA2751156A1 Visfatin therapeutic agents for the treatment of acne and other conditions The present disclosure relates to compositions and methods for treating acne and other conditions. In particular, the compositions and methods are useful for the treatment of sebum associated conditions.
EP2725029A1 New antibacterial compounds and biological applications thereof The invention relates to compounds of formula (I) wherein, - A1 and A2, identical or different, are H, (C1-C6) alkyl, (C1-C6) fluoroalkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, (C1-C6) alkyl-ORa, (C1-C6) alkyl-SRa, (C1-C6) alkyl-NRaRb, ORa, SRa, NRaRb, or CORa; - A3 is H, OH or form a carbonyl with A4; - A4 is H, OH or form a carbonyl with A3; - A5 is H, OH, CRaRbOH or F; - A6 is H or F; - X is CH2, CHF, CF2, CHOH, O, S, NRa or a simple bond; - Y is P(O) (ORa) (ORb) or P(O) (ORa) (NRaRb) ; - V is O or S; - A7 is H, (C1-C6) alkyl, (C1-C6) fluoroalkyl, (C2-C6) alkenyl, (C2-C6) alkynyl or (C1-C6) alkyl-ORa; - Ra and Rb, identical or different, are selected from the group consisting of H, (C1-C6) alkyl, (C1-C6) fluoroalkyl, (C1-C6) alkyl-OH and (C1-C6) alkyl-O-(C1-C6) alkyl; and their addition salts thereof with acids and bases, their preparation and their use in the antibacterial prevention and therapy, used alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity.
US7687536 Aminocycloalkyl cinnamide compounds for arrhythmia and as analgesics and anesthetics Aminocycloalkyl cinnamide compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of local analgesia and anesthesia.
CN101921245A Sulfonamides compound for inhibiting carbonic anhydrase II and synthesis method and application thereof The invention relates to a sulfonamides compound for inhibiting carbonic anhydrase II and a synthesis method and an application thereof. The compound has the structure as shown in the specification. The invention features economical and reasonable synthetic route and high utilization of resources. The synthesis method is simple and easy to carry out and is more suitable for large-scale industrialized production. With human carbonic anhydrase II (Human Carbonic Anhydrase II, hCA II) expressed by procaryotic cell as an enzyme source, the invention establishes an in-vitro carbonic anhydrase inhibitor screening model. In addition, the compound of the invention has inhibitive effect on activity of the human carbonic anhydrase II.
US7842822 (3aS, 4S, 9bS)-4-(4-Hydroxy-phenyl)-1,3a,4,9b-tetrahydro-3H-2,5-dioxa-cyclopenta[a]naphthalen-8-ol, used for the treatment of benign prostatic hyperplasia, cardiovascular diseases, neurodegenerative disorders, incontinence, nervous system disorders, gastrointestinal disorders and osteoporosis The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof useful as Estrogen Receptor beta agonists for treating Estrogen Receptor beta mediated diseases such as benign prostatic hyperplasia.
WO2008139261A9 Omega-3 lipid compound The present invention relates to a lipid composition comprising at least omega-3 polyunsaturated alcohols, or pro-drugs thereof, which omega-3 polyunsaturated alcohols, or pro-drugs thereof, comprising at least (all-Z)-5,8,11,14,17-eicosapentaen- 1-ol, or pro-drug thereof, and (all-Z)-4,7,10,13,16,19-docosahexaen-1-ol, or pro-drug thereof, and their use as a pharmaceutical, in particular for the treatment of elevated triglyceride levels. The invention also relates to methods for the preparation of these pro-drugs from marine oils.
US20110008432 Method for Treating a Patient in Need of Aspirin Therapy The present disclosure is directed to a method for treating a disease or disorder in a patient at risk of developing an NSAID-associated ulcer by administering to the patient in need thereof a pharmaceutical composition in unit dosage form comprising aspirin, or a pharmaceutically acceptable salt thereof, and an acid inhibitor to the at risk patient and thereby decreasing the patient's risk of developing an ulcer.
US20050032777 benzyl carbamates and ureas such as 5-(4-(4-cyclopropylmethylpiperazine-1-carbonylaminomethyl)-3-methylbenzoyl)-1-methyl-4,10-dihydropyrazolo[5,4-b][1,5]benzodiazepine, used for treatment of sexual disorders Compounds according to general formula (1), wherein G1 is NR5R6 or a fused polycyclic group are novel. They are selective and potent oxytocin agonists. Pharmaceutical compositions of such compounds are useful in the treatment of, inter alia, erectile dysfunction.
CN103349674A Tortoise shell rana japonica oil composition for increasing bone density and preventing osteoporosis The invention discloses a tortoise shell rana japonica oil composition for increasing bone density and preventing osteoporosis. The tortoise shell rana japonica oil composition is characterized by consisting of rana japonica oil, tortoise shell glue, tortoise shell calcium, icariin and cucumber seed extract. The synergistic effect of each component is utilized for preparing the components into oral preparation, for example, hard capsules, soft capsules, tablets, granules, powder, pills, tea bags and medicinal liquor. The composition can be applied to Chinese patent medicine or health-care food, and has the effect of preventing osteoporosis.
CN103585151A Famotidine and dexibuprofen compound tablets and preparation method thereof The invention provides famotidine and dexibuprofen compound tablets and a preparation method thereof. The compound tablets consist of dexibuprofen, famotidine, a disintegrating agent, a diluent, a lubricant and a glidant, wherein the weight ratio of the famotidine to the dexibuprofen is 1: (29-31). The preparation method comprises the following steps: the famotidine is mixed with the diluent and the disintegrating agent, and is added with adhesive for palletizing by the wet method, then is dried to prepare famotidine particles; the dexibuprofen is mixed with the diluent and the disintegrating agent to prepare dexibuprofen particles; the famotidine particles are mixed with the dexibuprofen particles evenly to obtain mixed particles I; the lubricant and the glidant are added in the mixed particles I for evenly mixing to obtain mixed particles II; and the mixed particles II are compressed to form the tablets. The famotidine and dexibuprofen compound tablets have the advantages of better curative effect, quicker effect achievement and small dosage, and can be directly taken orally to treat adult rheumatic arthritis and osteoarthritis.
CN1566136A Pasqueflower notoginsenosides and extraction method, medicinal uses and pharmaceutical preparation thereof The invention provides a Chinese bulbul total saponin and method for extraction which comprises, charging right amount of alcohols into Chinese bulbul, heating for convection flow, collecting and combining the extract liquid, removing impurities from the extract, filtering, feeding the filter liquor into acid and alkali treatment big hole adsorption resin column, washing the columns with deionized water until the eluate becomes achromatic, conducting elution with alcohols, reclaiming alcohol eluent through decompression, evaporating to dryness.
US20110286945 Compounds, Formulations and Methods for Reducing Skin Wrinkles, Creasing and Sagging Methods, compounds, and topical formulations for reduction of skin sagging, creasing and/or wrinkling are disclosed. The methods comprise topically applying a composition comprising an α2 adrenergic receptor agonist. Amelioration of skin sagging, creasing and/or wrinkling begins within minutes after topical application of a disclosed composition. A single application can significantly reduce skin sagging, creasing and/or wrinkling for at least about 8 hours.
CN101081861A Glycyrrhizic acid double salt and preparation thereof The present invention relates to medicine technology, and is especially one kind of complex glycyrrhizinate and its preparation process. The complex glycyrrhizinate has the liver protecting effects of glycyrrhizic acid or glycyrrhizinate and essential phospholipids combined together, and thus hepatosis treating effect higher than that of each of glycyrrhizic acid or glycyrrhizinate and essential phospholipids.
EP0732924B1 Tts containing a parasympathomimetic and a parasympatholytic agent A transdermal therapeutical system for preventing or pretreating poisoning by highly toxic organophosphoric neurotoxins is characterised in that it contains a pharmaceutical composition with a combination of active substances that includes at least one parasympathomimetic agent and at least one parasympatholytic agent.
CN1958597A Triterpene saponin compound of cycro jackfruit alkyl, and effect for anti tumor This invention relates to a cycloartane triterpenoid compound and its anti-tumor applications. The compound, with a general chemical formula shown in formula I, has in vitro anti-tumor activity. The compound and its derivatives can be used to manufacture anti-tumor drugs.
US20100136002 Methods for treating and preventing multiple sclerosis We have discovered that LRG-47 (also called p47 GTPase), plays a central role in the pathogenesis of multiple sclerosis, and that inhibition of LRG-47 activity by anti-LRG-47 antibodies or of LRG-47 expression by siRNA dramatically reduce the pathology and symptoms of multiple sclerosis. Certain embodiments of the invention are directed to the therapeutic use of anti-LRG-47 antibodies (mouse or rabbit or other antibodies that are humanized or human antibodies to LRG-47, preferably antibodies made against human LRG-47) or siRNA or antisense nucleotides that specifically hybridize with the gene or mRNA or cDNA encoding human LRG-47 to treat or prevent multiple sclerosis and other autoimmune diseases that are T-cell-mediated. Other embodiments are directed to methods for the diagnosis of multiple sclerosis or to determining the aggressiveness of multiple sclerosis by determining the amount of human LRG-47 or LRG-47 mRNA in a biological sample from the patient.
WO2012076667A1 Compounds for treatment of heart failure A combination of: a first tetracycline (TC) component; and a second component capable of releasing nitric oxide (NO) or a nitrate capable of mimicking NO effects in vivo (NO mimetic). The combinations of the invention advantageously act as more effective MMP modulators with selective reductions in circulating MMP-9 levels in-vivo and inhibitory effects on MMP-2 and MMP-9 levels in-vitro. The combinations of the invention also advantageously act as modulators of inflammation mediators. The co-existence of abnormalities of MMP enzymes and inflammation in many diseases make these characteristics advantageous. Therefore, the various combinations of the invention find utility in medical applications where MMPs and/or inflammation is implicated.
CN1833649A Jixuedai gel with action of promoting wound reunion, and prepn. thereof A gel of asiaticoside for promoting healing of wound and treating burn, wound, skin ulcer, scleroderma, etc is prepared from asiaticoside and proper auxiliary. Its preparing process is also disclosed.
CN102429884A Methylphenidate hydrochloride oral cavity disintegrating pharmaceutical composition The invention provides a methylphenidate hydrochloride oral cavity disintegrating pharmaceutical composition which has good stability, high bioavailability and low cost, can be industrialized, can be better applied clinically and has more obvious advantages.
CN103536619A Amoxicillin sodium and clavulanate potassium composition powder for injection The invention discloses an amoxicillin sodium and clavulanate potassium composition powder for injection, and belongs to the field of medicine and medicine preparation technology. The amoxicillin sodium and clavulanate potassium composition powder comprises following raw material ingredients, by weight, 7.26 to 9.17 parts of amoxicillin sodium and clavulanate potassium, 5.93 to 7.67 parts of chitosan nanoparticle, and 81.38 to 87.10 parts of injection water. Advantages of the amoxicillin sodium and clavulanate potassium composition powder are that: medicine water solubility is increased, and excellent medicine stability is ensured; the nanoparticle medicine carrier is capable of changing membrane transport mechanisms, and increasing medicine permeability against biological membranes, and is beneficial for exhibition of pharmacological functions in cells; it is shown by long-term experiment of stability that the amoxicillin sodium and clavulanate potassium composition powder can be stored for 2 years at a temperature of 30 DEG C, and medicine stability and clinical medicine safety in transporting be ensured; amoxicillin sodium and clavulanate potassium coated by the nanoparticle carrier are rapidly gathered at primary organs, such as liver and spleen, in the reticuloendothelial system along veins, so that toxicity caused by nonspecific gathering of medicine is reduced; and the chitosan nanoparticle can be used as a freeze-dried skeleton agent of the freeze-dried powder injection instead of mannitol so as to avoid active effects of mannitol on human bodies.
US8623862 Derivatives of N-[(1H-pyrazol-1-yl)aryl]-1H-indole or 1H-indazole-3-carboxamide, preparation thereof and applications thereof in therapeutics The present invention relates to compounds corresponding to formula (I): X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.
US6921650 Recombinant methods and materials for producing epothilone and epothilone derivatives Recombinant nucleic acids that encode all or a portion of the epothilone polyketide synthase (PKS) are used to express recombinant PKS genes in host cells for the production of epothilones, epothilone derivatives, and polyketides that are useful as cancer chemotherapeutics, fungicides, and immunosuppressants.
WO2008109724A3 Treatment of cocaine-induced fetal brain injury A Disclosed is a method of therapeutically or prophylactically treating a pregnant mother for cocaine-induced fetal brain injury comprising administering a therapeutically or prophylactically effective amount of a cytochrome P450 inhibitor or prodrug thereof to the mother. Also disclosed is a method of screening for inhibitors of cocaine-induced fetal brain injury. Uses of compounds and compositions to manufacture a medicament for treating a pregnant mother for cocaine-induced fetal brain injury are further provided.
CN102018777A Formula for treating psoriasis and preparation method thereof The invention discloses a formula for treating psoriasis, which comprises the following components in percentage by weight: 15 to 20 percent of kusnezoff monkshood, 30 to 38 percent of realgar, 30 to 40 percent of sulfur and 15 to 22 percent of root bark of the peony tree. A method for preparing the formula for treating the psoriasis comprises the following steps of: grinding 15 to 20 percent of kusnezoff monkshood, 30 to 38 percent of realgar, 30 to 40 percent of sulfur and 15 to 22 percent of root bark of the peony tree into fine powder and putting into a container. During use, 3 to 5 grams of fine powder is taken out and packaged by gauze, and the gauze bag is dipped with 80 percent alcohol for application. The invention has the advantages that: the formula for treating the psoriasis is convenient to use, and the treatment effect is improved.
WO2007114475A1 Cocrystal of c-glycoside derivative and l-proline A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. This cocrystal ensures a constant quality, excelling in storage stability, and does not exhibit any moisture absorptivity, being a cocrystal of known compound (A) being suitable as a crystal of raw drug to be finished into pharmaceutical products.
CN101007834A Nucleic acid molecule RTN4BSR4 and its application in preparing anticancer medicine The invention belongs to the field of biological pharmacology, and relates to the use of RTN4BSR4 in preparing antitumor medicament, wherein a nucleotide molecule RTN4BSR4 is provided which can be used for preparing antitumor medicaments, the sequence of the molecule includes 5'-GGAGCACUACCAUCUGUUU-3', 5'-GGAGCACTACCATCTGTTT-3', 5'-AAACAGATGGTAGTGCTCC or 3'-AAACAGAUGGUAGUGCUCC-5'. Compared with nude mice containing no RTN4BSR4, the tumor growth of the nude mice containing RTN4BSR4 is inhibited appreciably, which is becoming more appreciable with lapses of time. The invention provides a novel approach for the treatment and alleviation of tumor.
EP2749558A1 Method for producing optically active naphthalene compound The present invention provides an industrially advantageous method for producing an optically active naphthalene compound useful as a therapeutic agent for dermatitis or the like. Specifically, the present invention provides a method for producing an optically active naphthalene compound [I], which comprises: a step of reacting a compound [a-1] and a compound [b-1] with each other in the presence of a base and a catalyst that is composed of a Pd compound and a tertiary phosphine ligand (step a); a step of asymmetrically hydrogenating a compound [c-1] in the presence of a hydrogen donor and a complex that is prepared from a ruthenium compound and a chiral ligand, or alternatively in the presence of an optically active oxazaborolidine compound (a CBS catalyst) and a boron hydride compound (step b); and a step of treating a compound [d-1] with a reducing agent (step c). (In the above formulae, Ra and Rb represent the same or different lower alkyl groups; and X1 represents a halogen atom.)
CN102526022A Application of epigallocatechin-3-gallate in preparation of antitumor drug The invention belongs to the fields of medicine and gene engineering, relates to a new medicinal application of epigallocatechin-3-gallate EGCG, and particularly relates to an application of epigallocatechin-3-gallate in the preparation of antitumor drugs. Cell experiments demonstrate that the epigallocatechin-3-gallate is a CYPJ inhibitor, and has the capability of inhibiting liver cancer cell growth; a large dose of EGCG basically has no toxicity to liver, kidney and heart. Experiment results also show that when EGCG is added into a culture solution of tumor cells, the proliferation of tumor cells is inhibited; the tumor cells are blocked at the G1 stage; the activity of CYPJ is inhibited; the activation of an Erk signal path by CYPJ protein is blocked. The epigallocatechin-3-gallate of the invention can be used for the preparation of antitumor drugs, especially anti-liver cancer drugs; and the drugs are designed aiming at cell target points, and drug resistance is not easy to generate.
US20080319072 Composition and method for treating bacterial, viral, fungal diseases, inflammation and pain The present invention is directed to compositions and methods of treating bacterial, viral, fungal diseases; inflammation or inflammatory-related disorders; pain; and skin conditions. The composition comprises an organic solvent extract, which is prepared by the method comprising the steps of: (a) mixing methionine with water, (b) adding an aqueous hypochlorite solution to the methionine solution and mixing, (c) adding a water-immiscible organic solvent to (b) and mixing, and (d) separating the organic solvent phase from the water phase to obtain the organic solvent extract. The present invention is also directed to a method for preparing the organic solvent extract.
US7771771 fatty acid esters of phytosterols and phytostanols; preparing an edible oil or fat blend with elevated sterol and/or stanol content comprising liquid vegetable oil and a sterol and/or stanol fatty acid ester composition This invention relates to phytosterols and phytostanols, in particular to fatty acid esters of phytosterols and phytostanols with a specified fatty acid composition. The invention further relates to methods for preparation of the phytosterol and phytostanol esters and their uses.
US20100311075 Human sodium-dependent bile acid transporter proteins A novel sodium-dependent bile acid transporter protein, an Na+/H+ exchange transporter protein, a P-type ATPase protein and a vanilloid receptor protein, and polynucleotides encoding these proteins are useful in screening preventives/remedies for hyperlipemia, arteriosclerosis, genital diseases or digestive diseases; respiratory diseases, renal diseases or digestive diseases; pancreatic diseases, central nerve diseases, digestive diseases or respiratory diseases; inflammatory diseases, rheumatoid diseases or diabetic neurosis; etc.
US8263634 Heteroaryl-ureas and their use as glucokinase activators This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
US20120065228 Compositions and methods for treating, controlling, reducing, or ameliorating ocular inflammatory with lower risk of increased intraocular pressure A composition for treating, controlling, reducing, or ameliorating inflammatory pain comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can comprise an additional anti-inflammatory agent and can be formulated for topical application, injection, or implantation. It may be used in a method of managing ocular inflammation and/or pain such that it has lower risk of eliciting increased intraocular pressure seen with glucocorticoids.
CN102382164A Toad lactam compound as well as preparation method and application thereof The invention discloses a toad lactam compound as well as a preparation method and application thereof. The preparation method comprises the steps of: mixing a toad lactone compound and ammonium acetate according to molar ratio of 1: (3-8); dissolving by utilizing organic solvent; reacting at a temperature of 100-160 DEG C for 0.5-3h under the protection of inert gas; decompressing, concentrating, removing the organic solvent; separating and purifying by utilizing a preparative high performance liquid chromatography method; and obtaining the toad lactam compound. The preparation method is simple, easy to carry out, safe, reliable and higher in yield. Proved by experiments, the toad lactam compound obtained in the invention has the advantages of good antitumor effect, very strong inhibitory action on various cancer cells such as PC3, DU145, LNCaP, MCF-7 and Hela, especially much better selective inhibitory action to hormone-dependent cancer cells such as the LNCaP and the MCF-7 than the toad lactone compound and remarkably lower toxicity to normal cells than the toad lactone compound. The toad lactam compound applied in preparing antitumor drugs has the advantages of being high in efficiency and low in toxicity and meeting the requirements of drug development.
CA2267309C Use of 1-hydroxy-2-pyridones for the treatment of skin infections Compounds of the formula I (see formula I) are suitable for the production of pharmaceuticals for the topical treatment of skin infections which are caused by fungi and bacteria.
EP1561815A2 Tissue-specific and target rna-specific ribozymes The invention provides tissue-specific and target RNA-specific ribozymes. These ribozymes can be used to destroy target-specific neoplasms and to treat viral infections, among other uses. The ribozymes of the present invention comprise a 5' autocatalytically cleaving ribozyme sequence, a catalytic ribozyme comprising a target RNA-specific binding site and a 3' autocatalytically cleaving ribozyme. The invention also provides nucleic acids which encode the ribozymes of the invention. These nucleic acids can be used to express the ribozymes of the invention at the selected site. Methods of treating disease by administering the ribozymes are provided.
US20130059774 Efflux pump inhibitors Novel compositions and methods of reducing microbial resistance to antimicrobial agents and treating infections are disclosed. In particular, compositions and methods of inhibiting efflux pump activity, treating infection and methods of enhancing antimicrobial activity of antimicrobial agents are provided.
US20120121695 Acoustically sensitive drug delivery particles comprising non-lamellar forming phosphatidylethanolamine Novel acoustically sensitive drug carrying particles comprising non-lamellar forming lipids are disclosed, as well as uses and methods thereof. The drug carrying particles accumulate in the diseased target tissue and efficiently release their pay-load upon exposure to acoustic energy.
WO2009019616A3 Isoprekinamycin analogs and syntheses thereof The present invention relates to the preparation of various benzo[α]fluorenes The benzo[α]fluorene moiety appears in a variety of natural products, some of which have been shown to exhibit anticancer and antibacterial effects Methods of the present invention provide facile access to some of these natural products as well as derivatives thereof.
CN101032497A Polyenylphosphatidylcholine freeze - dried powder injection for injecting and the preparing method thereof The present invention is freeze dried Essentiale phospholipids powder for injection and its preparation process. The freeze dried Essentiale phospholipids powder for injection consists of Essentiale phospholipids in 0.1-0.5 weight portions, alkaline material in such amount of regulating the pH value to 5.0-9.0, and excipient in 0.002-0.7 weight portions. The medicine of the present invention is used in treating acute and chronic liver diseases, psoriasis, radiation syndrome and other diseases.
CN101879267A Compound tincture for treating foot helosis The invention discloses a compound tincture for treating foot helosis, which has the advantages of good treatment effect, no side effect, toxicant elimination, inflammation diminishing, sterilization, repair and reactivation of skin cells and achieves the effect of addressing both the symptoms and root causes by promoting the microcirculation of epidermis to make skin become fine and smooth. The compound tincture is prepared from 10 to 20 weight parts of salicylic acid, 10 to 20 weight parts of java brucea fruit, 10 to 20 weight parts of gentiana macrophylla pallac, 10 to 20 weight parts of Chinese honeylocust spine, 10 to 20 weight parts of honeysuckle, 10 to 20 weight parts of lithargite, 8 to 15 weight parts of camphor root, 8 to 15 weight parts of grosvenor's momordica leaf, 8 to 15 weight parts of podocarp root, 8 to 15 weight parts of vietnamese sophora root, 8 to 15 weight parts of eggplant root, 4 to 8 weight parts of calomel, 4 to 8 weight parts of clematis root, 4 to 8 weight parts of Chinese gall, 4 to 8 weight parts of cortex pseudolaricis, 4 to 8 weight parts of angelica dahurlica, 1 to 5 weight parts of ligustrum leaf, 1 to 5 weight parts of houttuynia cordata thunb., 1 to 5 weight parts of eriocarpous glochidion leaf, 1 to 5 weight parts of aloes, 1 to 5 weight parts of peppermint oil and 150 weight parts of absolute ethyl alcohol through compatibility.
WO2009154460A1 Modulation of memory function. The invention relates to means and methods for modulating memory function. In particular, the invention provides a method to enhance or facilitate memory retrieval, in particular for the treatment of Alzheimer. Provided is a method of modulating memory retrieval in a mammalian subject, comprising administering to the subject a composition comprising an effective amount of an agent capable of modulating the activity of exchange proteins directly activated by cAMP (Epacs).
WO2007124545A1 Integrase inhibitors - 2 The present invention provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Compounds of formula (I) are also provided.
WO2007094669A2 Composition used as a nutritional supplement and medication for the treatment of degenerative visual disorders and inflammation The invention relates to a composition and a dosing unit which can be used as nutritional supplement or as medication for the treatment of retinitis pigmentosa (RP). The composition comprises a combination of lutein, zeaxanthin, glutathione and alpha lipoic acid, optionally supplemented with an extract of Lucium Barbarum Lynn. This composition inhibits the death of photoreceptors as a consequence of RP, whereby the visual faculties of the patient are retained for a longer time. The composition is also useful as an anti-inflammatory drug.
WO2013079501A1 Crystalline dapagliflozin hydrate The present invention is directed to crystalline dapagliflozin hydrate and a process for obtaining the same. Dapagliflozin has the structure of formula (I).
EP2049544B9 Purinone derivatives as hm74a agonists The present invention relates to purinone derivatives of formula I which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.
US20110257080 Hepatitis B Virus Compositions and Methods of Use A polypeptide comprising a preS1 region of hepatitis B virus (HBV), or a fragment thereof, and/or the preS2 region of HBV or a fragment thereof, and methods of use to inhibit virus infection are disclosed. A lentivirus comprising hepatitis B virus (HBV) envelope proteins, or a fragment thereof, and/or the L envelope protein of HBV and/or the M envelope protein of HBV or a fragment thereof, and/or the S envelope protein of HBV or a fragment thereof, and methods of use of this lentivirus HBV pseudovirus as a gene therapy to target hepatocytes for the administration of therapeutic agents are also disclosed.
CN103012434A Cefathiamidine compound crystal and preparation method as well as pharmaceutical composition thereof The invention relates to a cefathiamidine compound crystal. The compound crystal is measured by adopting a powder X-ray diffraction measurement method, and X-ray powder diffraction atlas expressed by a diffraction angle of 2 theta plus or minus 0.2 degrees shows a feature diffraction peak at 10.3 degrees, 10.6 degrees, 14.9 degrees, 16.9 degrees, 17.9 degrees, 20.2 degrees, 20.8 degrees, 26.7 degrees, 29.8 degrees and 30.5 degrees. The compound crystal is a new crystal form different from the cefathiamidine crystal form of the prior art, and proved by stability test, the compound crystal has excellent stability. Simultaneously, the invention also provides a preparation method of the cefathiamidine compound crystal as well as the pharmaceutical composition containing the compound crystal.
WO2008011080A3 Benzo(d) isoxazole derivatives as c-kit tyrosine kinase inhibitors for the treatment of disorders associated with the over production of histamine The present invention comprises a new class of compounds capable of modulating the c-kit protein kinase and, accordingly, useful for treatment of c-kit mediated diseases including, without limitation, autoimmune disease, allergies, mastocytosis, mast cell related tumors and various fibrotic diseases. The compounds have a general Formula (I) wherein R1-5, X, Y and Z are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
US20080160082 Controlled release compositions comprising Nimesulide A controlled release pharmaceutical composition for peroral administration including a single unit fast release fraction and a single unit extended release fraction which includes nimesulide as an active drug upto 99% w/w of the composition, one or more release controlling materials from 0.1% to 99% w/w of the composition and pharmaceutical excipients from 0% to 90% w/w of the composition. The nimesulide is present in the fast release fraction and in the extended release fraction.
US20110250211 Variable domains of camelid heavy-chain antibodies directed against glial fibrillary acidic proteins The present invention relates to the use of variable domains of camelid heavy-chain antibodies (VHH domains) directed against an intracellular target and having an isoelectric point of at least 8.5, for targeting said intracellular target or for the preparation of a peptide vector. Particularly, it concerns VHH domains directed against a glial fibrillary acidic protein and uses thereof for preparing therapeutic or diagnostic agents.
CN101780203B Lubrication effervescent agent for yin nourishing, nest warming, body deodorizing and youth keeping and preparation method thereof The invention relates to a lubrication effervescent agent for yin nourishing, nest warming and a preparation method thereof. The lubrication effervescent agent mainly comprises a major agent, a minor ingredient and a disintegrant, wherein soybean isoflavone is used as the major agent and accounts for 30-60 percent of the effervescent agent, mannite is used as the minor ingredient and accounts for 15-30 percent of the effervescent agent, and sodium bicarbonate is used as the disintegrant and accounts for 20-50 percent of the effervescent agent. The preparation method of the invention comprises the following steps: fully soaking and mixing the soybean isoflavone and gingerol in medical alcohol, mixing the mixture prepared in the first step with other components of the major agent, mixing the mixture prepared in the second step with the minor ingredient and the powdered disintegrant, and preparing tablets, powder and granules. The invention has the significant advantages of nourishing yin, warming the nest, keep youth, deodorizing the body, delay aging and preventing and easing menopausal symptoms.
US20080200526 N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine; allergic rhinitis, asthma, allergic conjunctivitis, allergic dermatitis, atopic dermatitis, contact dermatitis and urticaria Disclosed herein is a composition for the treatment and prevention of allergic inflammatory diseases comprising N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salts. The composition exhibits excellent medicinal effects on allergic inflammatory diseases, with a great reduction in typical chronic inflammation symptoms, such as an increase of eosinophil level in bronchoalveolar lavage fluid, total leukocyte level and eosinophil level in blood, the hypertrophy or hyperplasia of bronchial epithelium due to an increase in the number of mucus cells, a reduction in alveolar surface area resulting from the hyptertrophy of alveolar walls, and the infiltration of inflammatory cells.
WO2008152423A3 Treatment of inflammation or autoimmune diseases with sulphated compounds The present invention relates to sulphated compounds containing one to twelve monosaccharide subunits, for the treatment or prevention of anon-gastrointestinal disease or conditionby gastrointestinal absorption, wherein none of the monosaccharide subunits is pyranosyl with N-substitution at the 2-position relative to the anomeric carbon of the pyranosyl subunit. The present invention also relates to corresponding methods of treating or preventing anon-gastrointestinal disease or condition. Additionally, the present invention relates to a method of modifying, or testing for a modification in,the level of a cytokine in vivo, ex vivoor in vitro, said method comprising contacting a sulphated compound with a cell, wherein the compound comprises at least one monosaccharide subunit. The present invention also relates to unit dosage forms comprising at least 2.5g of any of the above compounds, to unit dosage forms comprising the molar equivalent of at least 1 g of any of the above compounds in theirfree acid and/or base form, and to unit dosage forms comprising any of the above compounds other than sucralfate.Preferred compounds of the present invention are sucrose octasulphate and sucralfate.
CN102240263A Tiapride hydrochloride injection and preparation method thereof The invention discloses a pharmaceutical preparation of a compound, namely a tiapride hydrochloride injection and a preparation method thereof. The preparation contains tiapride hydrochloride, sodium chloride, a phosphate buffer (pH 7.8) and water for injection. The method comprises the following steps of: taking proper amounts of water for injection, sodium chloride and tiapride hydrochloride, adding the tiapride hydrochloride and the sodium chloride to the water for injection, dropwise adding the phosphate buffer (pH 7.8) while stirring until the pH value of the solution is 4.0-6.0, continuously stirring until fully dissolved, adding activated carbon which is 0.1% (g/ml) of the total volume of the solution, stirring for 30 minutes, filtering, adding water to full dose, filtering, filling, sterilizing, inspecting by a lamp and packing. The invention has the characteristics of simple formula and process, high production efficiency, good stability of the liquid medicine and the like.
WO2009089338A2 Method and compositions for administering resveratrol and pterostilbene Resveratrol and/or pterostilbene are added to a chewable carrier, to enhance absorption of resveratrol and/or pterostilbene buccally or through the mucous membranes of the mouth. The composition containing the resveratrol and/or pterostilbene is designed to be retained in the mouth for at least 20 seconds and up to 20 minutes to ensure absorption of the resveratrol and/or pterostilbene through the mucous membranes of the mouth.
EP1941871A1 Formulations for prevention and treatment of breast cancer with 4-hydroxy tamoxifen The present invention provides methods for treating and preventing breast cancer by administering 4-hydroxy tamoxifen to a patient. It also provides pharmaceutical compositions of 4-hydroxy tamoxifen suitable for percutanous administration. When percutaneously administered to a patient's breasts, 4-hydroxy tamoxifen concentrates locally, and exerts an anti-estrogenic effect. In patients with breast cancer, this effect reduces tumor tissue proliferation. In patients at risk for developing breast cancer, the anti-estrogenic effect prevents breast tumor formation.
CN102429859A Preparation method of diphenhydramine cream The invention discloses a preparation method of diphenhydramine cream, and the product belongs to the pharmaceutical field. The cream has antianaphylaxis and antipruritic effects and used for treating allergic and itching skin diseases. The formulation raw materials used for preparing the cream comprise diphenhydramine, tween 80, glyceryl monostearate, liquid paraffin, ethyl hydroxybenzoate, glycerol, sodiumdodecylsulfate, ethylparaben and purified water, wherein the function of the tween 80 is emulsifying agent, the function of the glyceryl monostearate is stabilizing agent and thickening agent, the liquid paraffin is matrix of ointment, the function of the ethyl hydroxybenzoate is antibacterial preservatives, the glycerol is a backing material, the sodiumdodecylsulfate is used as pasty foaming agent, and the ethylparaben is pharmaceutical excipient having a certain preservative effect. The preparation method is simple, the used material is cheap, the production cost is low, and the use effect is good through practice tests.
WO2007035405A3 In-vivo and in-vitro method for detecting amyloid deposits having at least one amyloidogenic protein An amyloid deposit can be detected by administering to a subject or applying to a sample a compound of Formula (I) or Formula (II) or structures 1-45, as described, and then imaging to detect binding of the compound to an amyloid deposit, where the amyloido genie protein of the deposit can be AL, AH, ATTR, Aβ2M, AA, AApoAI, AApoAII, AGeI, ALys, AFib, ACys, ABri, ADan, APrP, ACaI, AlAPP, AANF, APro, AIns, AMed, AKer, A(tbn), and/or ALac.
CN101279028A Oral liquid vaccine for preventing and controlling avian influenza of domestic animals and domestic birds and method of preparing the same The invention relates to a veterinary pharmaceutical composition and a preparation method thereof. The veterinary pharmaceutical composition of the invention is a vaccine oral solution for the prevention and the treatment of bird flu of domestic animal and fowl, and is prepared by the raw materials according to the following parts by weight: 10 to 20 parts of forsythia suspensa, 10 to 25 parts of asarum, 5 to 20 parts of ilex pubescens, 15 to 30 parts of rhizoma anemarrhenae, 8 to 20 parts of wild chrysanthemum, 10 to 20 parts of polygalae, 10 to 25 parts of lobelia chinensis, 2 to 5 parts of snake galls, 10 to 25 parts of ox to gall, 40 to 60 parts of aloe, 25 to 40 parts of rock sugar, 5 to 15 parts of rimantadine and 3 to 10 parts of azithromycin. The oral solution of the invention can be directly used as daily feed for feeding domestic animals and fowl, which can effectively inhibit bird flu virus, reduce the infection rate of respiratory tract and lung and prevent domestic animal and fowl from being infected by bird flu.
WO2010117296A1 Agent for preventing influenza and acute respiratory diseases The invention relates to the chemical and pharmaceutical industry, namely, to the production of an agent that is used for preventing influenza and acute respiratory diseases and is based on substances isolated from raw vegetable matter. The proposed agent for preventing influenza and acute respiratory diseases is characterised in that it is a mixture of dihydroquercetin, arabinogalactan and ascorbic acid with the following mass ratio of the respective ingredients - 1:(16-18):1. The agent can be in the form of a pill. Clinical and epidemiological studies of the claimed agent show that the agent is well tolerated and does not give rise to side effects, allergic reactions or complaints relating to the functioning of the gastrointestinal tract and other systems of the body.
US20120201862 Process for the preparation of colloidal systems for the delivery of active compounds The present invention relates to a process for the preparation of colloidal systems, such as nanocapsules and nanoparticles, which incorporates a homogenization step for reducing particle size.
CN103110581A Taxol microemulsion drug composition and preparation method thereof The invention discloses a taxol microemulsion drug composition and a preparation method thereof. The drug composition comprises the following active ingredients: taxol, an oil phase, a solubilizing agent, a stabilizing agent, an excipient, an acidity regulator and water for injection and is characterized in that the main grain size of taxol microemulsion ranges from 10nm to 40nm; and the parts by weight of taxol, an emulsifying agent, the oil phase and the water phase are respectively 30, 1500-3000, 100-350 and 5000-50000. The drug composition has the beneficial effects that taxol is taken as the main drug and different auxiliary materials are added to prepare microemulsion; the taxol microemulsion freeze-dried preparation prepared through freeze drying has good water solubility and stability; the clinical defect of severe allergic reaction of the taxol injection in the market is overcome; meanwhile, the preparation process is simple and is suitable for industrial mass production; and a new administration dosage form is provided for clinical application of taxol.
CN103110572A Gynecological antimicrobial gel recipe and preparation method thereof The invention discloses a gynecological antimicrobial gel recipe and a preparation method thereof. A gel takes chitosan-iodine as a main active ingredient and comprises raw materials of chitosan-iodine, glacial acetic acid, polysorbate-20, glycerin, potassium iodate, chitosan, hydroxyethyl cellulose and purified water. The preparation method comprises the following steps of: (1) weighing according to the recipe for standby; (2) adding the glacial acetic acid, the polysorbate-20, the glycerin and part of the purified water into the chitosan-iodine to be fully and uniformly mixed, and completely dissolving for standby; (3) taking a small amount of purified water to dissolve the potassium iodate, adding the dissolved potassium iodate into standby materials to be mixed, and stirring uniformly; (4) adding the chitosan according to the raw material mass ratio, and stirring to dissolve the chitosan; and (5) adding the hydroxyethyl cellulose according to the raw material mass ratio, adding the residual purified water to 100% and slowly stirring to form the gel. The gel has the advantages of good stability, excellent sterilization effect and convenience in use; and the processed gel can be used for treating colpitis mycotica, mixed vaginitis and the like as well as chronic cervicitis.
US7335727 fusion inhibitor; high stability and high valence; higher efficacy, and lower administration dosage, and thereby lower toxicity. A fusion inhibitor used to treat HIV infection, has an amino acid sequence as follows: X-SWETWEREIENYTKQIYKILEESQEQQDRNEKDLLE-Z, wherein X is either an amino group or -X1-X2, wherein X1 is an imino group, and X2 is either an acetyl group, a hydrophobic group, or a macromolecular carrier group; Z is a carboxyl group or -Z1-Z2, wherein Z1 is a carbonyl group, and Z2 is either an amino group, a tert-butyloxycarbonyl group, a hydrophobic group, or a macromolecular carrier group. This inhibitor has strong inhibitory activity against HIV infection.
CN101810565A Tolterodine gel preparation and preparation method thereof The invention discloses a tolterodine gel preparation, which is mainly prepared from free alkali tolterodine, gel matrix, film-forming matrix, organosilicon elastic body, percutaneous penetration accelerators, pH regulators, humectants, and the like. During use, the gel preparation contains the film-forming matrix which can form a flexible film after being dried, and can be externally coated on the thigh, the belly, the upper arm or shoulder, and other parts; flexible and wear-resistant thin film can be rapidly formed in the selected skin region; the gel is prevented from being taken away by the clothes; and meanwhile, the application site is in an unsealed state and has good air permeability. The contained organosilicon elastic body can obviously improve the dispersibility, flexibility, wettability, glossiness, and other performances of the gel system. The prepared gel is smooth, crystal clear and fine, has no foreign body sensation on the skin after use, durable medicament and slow release, good percutaneous absorption effect, convenient use, and improves the patient compliance.
CN102973736A Ointment for whitening skin The invention discloses an ointment for whitening skin. The ointment for whitening skin comprises: by weight, 50 to 60 parts of powdered stalactite, 10 to 15 parts of largehead atractylodes rhizome, 10 to 15 parts of rhizoma typhonii, 12 to 15 parts of dahurian angelica root, 10 to 12 parts of common aucklandia root, 15 to 18 parts of ass hide glue and 15 to 20 parts of mung bean flour. The ointment for whitening skin has effects of maintaining beauty and keeping young, invigorating blood circulation and dredging collaterals, improving skin blood circulation, making the skin shell pink and naturally whitening.
CN103006912A Method for preparing medicine capsule for clearing away heat and loosing bowels and dispelling rheumatism to relieve pain The invention discloses a method for preparing a medicine capsule for clearing away the heat and loosing the bowels and dispelling the rheumatism to relieve pain. The method comprises the following steps of: (1), an extraction process: 1, preparing materials and weighing, 2, extracting volatile oil, 3, preparing clear paste by taking cape jasmine fruits, licorice roots and chastetree fruits (fried), 4, percolating and 5, mixing; (2) a powder making process: 1, preparing the materials and weighing, 2, sterilizing, 3, drying and 4, pulverizing; and (3), a preparation process: 1, preparing the materials and weighing, 2, pelleting, 3, finishing granules, 4, totally blending, 5, filling and 6, polishing. When crude medicinal materials are extracted, the weight ratio of coptis chinensis to fructus forsythia to mint to inula flower to baical skullcap roots to schizonepeta to cape jasmine fruits to divaricate saposhnikovia roots to golden cypress to chrysanthemum to fructus viticis (fried) to licorice roots to szechuan lovage rhizome to rheum officinale to gypsum to platycodon grandiflorum to angelica root to dextrin to magnesium stearate is 5:40:20:10:40:40:40:20:20:80:40:20:20:160:20:40:40:30:2.8. The method has the advantage that the medicine capsule with good quality is produced.
CN101278943B Externally-applied medicine for curing psora The invention discloses a medicine, more particularly, a medicine for external application used for treating scabies and a preparation method thereof. The medicine for external application used for treating scabies is characterized in that the medicine is made by medicine materials with the weight parts as follows: 95 to 105 parts of sulfur and 4 to 7 parts of crinis carbonisatus. The preparationmethod of the invention is as follows: the sulfur is melted by low fire; the crinis carbonisatus is added; the sulfur and crinis carbonisatus are evenly mixed; and then solution is poured into a plurality of circular porcelain dies with the radius and thickness of 1cm; after being cooled, the solution is taken out and is put into a vessel filled with child urine to be soaked; the medicine is completely submerged in the child urine for seven days; afterwards, the medicine is taken out and dried to be packed into a case; and at last the medicine is made. The medicine needs a small amount of rawmaterial and the preparation method is simple. When in use, the medicine is applied to the surface of an afflicted part and is easy to be handled. Healing time is only four to six days, so the medicine achieves quick effect. In addition, cure rate reaches 100 percent and the medicine has no adverse effect.
US7125563 Sustained release pharmaceutical preparations and methods for producing the same An extended release tablet comprising a core including albuterol sulfate and extended release agent; and an extended release coating on the core to provide for sustained release of the albuterol sulfate.
EP2324035A1 Substituted n-phenyl-2,3-dihydroimidazo[2,1-b]thiazole-5-sulfonamide derivatives as 5-ht6 ligands The invention relates to compounds having pharmacological activity towards the 5-HT6 receptor, and more particularly to some N-phenyl-2,3-dihydroimidazo[2,1- b]thiazole-5 -sulfonamide derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT6 is involved.
WO2014008379A3 Diamine and meglumine salt forms of fatty acids Provided herein are diamine salts of eicosapentaenoic acid and docosahexaenoic acid, processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and the uses of such compounds as agents for treating dyslipidemia, cardiovascular diseases such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke and obesity.
CN102525967A Entecavir oral solid composition and preparation method thereof The invention discloses an entecavir oral solid composition prepared with dry granulating and a preparation method thereof. The entecavir oral solid composition disclosed by the invention comprises entecavir, a dispersing agent, a disintegrating agent and a lubricating agent; the particle size of the entecavir is controlled in a certain range by micronizing; the entecavir is uniformly dispersed in the composition; and the entecavir oral solid composition is prepared with dry granulating. The entecavir oral solid composition has a simple preparation method, is easy to control, and is suitable for large-scale industrial production; and a prepared product has uniform content and high stability.
US7196080 Respiratory system disordeers; chronic obstructive pulminary disease The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein R1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like, R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like, R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, and n: 0 or 1).
US20070254959 Oxidizing 3-(2-methoxy-5-methylphenyl)-3-phenylpropanol to produce 3-(2-methoxy-5-methylphenyl)-3-phenylpropanal, reacting with diisopropylamine in presence of a reducing agent, removing hydroxyl protecting group to obtain for obtaining 3-(2-hydroxy-5-methylphenyl)-N,N-diisopropyl-3-phenylpropylamine The process comprises reacting a compound of formula (II), where R is a hydroxyl protecting group, and the asterisk indicates an asymmetric carbon atom, with diisopropylamine in the presence of a reducing agent; optionally converting the resulting intermediate into a salt and, if so desired, isolating it; removing the hydroxyl protecting group; and if so desired, separating the desired (R) or (S) enantiomer, or the mixture of enantiomers and/or converting the obtained compound into a pharmaceutically acceptable salt thereof. Tolterodine is a muscarinic receptor antagonist useful in treating urinary incontinence and other symptoms of urinary bladder hyperactivity.
CN101279956A Matrix metalloprotease inhibitors and synthetic method thereof The invention discloses matrix metalloproteinase inhibitors with general formula(I) and synthesis method thereof. The invention has the advantages that the compounds are all micro-molecular quasi-peptide compounds; the synthesis process is short, the material is easy to get, and the production cost is low.
US7192611 Administering a Free-B-Ring flavonoid as cyclooxygenase-2 (COX-2) inhibitor to treat osteoarthritis, rheumatoid arthritis, menstrual cramps, Systemic Lupus Erythromatosis, psoriasis, migraines, inflammatory bowel disease, cancer The present invention provides a novel method for inhibiting the cyclooxygenase enzyme COX-2. The method is comprised of administering a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids to a host in need thereof. The present also includes novel methods for the prevention and treatment of COX-2 mediated diseases and conditions. The method for preventing and treating COX-2 mediated diseases and conditions is comprised of administering to a host in need thereof an effective amount of a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids and a pharmaceutically acceptable carrier.
EP0641218B2 Use of angiotensin antagonist (at1) for reducing post myocardial infarct mobidity and mortality The invention involves a method for treating a human survivor of a heart attack and provides further improvement in survival following the heart attack by the early initiation and long-term administration of a renin-angiotensin system inhibitor, preferably an angiotensin converting enzyme inhibitor. The inhibitor may be used on its own, or in conjuction with other therapeutic compounds such as β blockers and thrombolytic agents. The preferred inhibitor is captopril.
WO2009004899A1 Sialidase inhibitor It is intended to provide a novel sialidase inhibitor capable of inhibiting the activity of sialidase present in Trypanosoma cruzi or the like. An N-acylneuraminic acid derivative in which an aromatic ring has been introduced at the 9-position and 2α-position has a strong inhibitory effect on the activity of sialidase. The invention is directed to the sialidase inhibitor comprising the N-acylneuraminic acid derivative (in the following formula, R1 and R2 each independently represent a substituent having an aromatic ring) or a pharmaceutically acceptable salt thereof. (I)
EP1845090A1 Amide compound and thrombopoietin receptor activator The present invention provides compounds usuful for prevention, treatment or allevation of diseases against which activation of the thrombopoietin receptor is effective. A compound represented by the formula (1): wherein A, B, R1, L1, R2, L2, L3, Y, L4, R3 and X are the same as defined in the description, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
EP2465847A1 Azetidinone compounds and medical use thereof Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R1, R2, R3, R4, R5and R6 are defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention.
US20080255216 Diaryltriazoles as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase-1 2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11&bgr;-hydroxysteroid dehydrogenase Type 1 enzyme (11&bgr;-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11&bgr;-HSD-1.
CN103181931A Povidone iodine five-compound disinfectant The invention relates to a povidone iodine five-compound disinfectant which comprises the following components in percentage by weight: 5-20 percent of povidone lodine, 0.1-10 percent of medical glycerin, 0.1-2 percent of citric acid, 0.1-1 percent of nonoxynol-10, 0.01-0.1 percent of sodium hydroxide and the balance of water for injection. The povidone iodine five-compound disinfectant can be used for producing povidone iodine compound wipes with different specifications, povidone iodine compound cotton swabs, povidone iodine compound spongy cushions, povidone iodine compound hand-washing brushes and the like; and after the products are specially treated or sterilized, the sterility and the safety of the products are fully ensured, and after being unpacked, the products can be directly used, so that the cross contamination and the infection in an intermediate link are avoided. The povidone iodine five-compound disinfectant has the advantages of small skin irritation, low toxicity, lasting action, and safety and convenience in use; the povidone lodine five-compound disinfectant basically has no irritation to tissues and is used for skin and mucosa disinfection, such as cleaning before operation, operative site and wound disinfection, and skin cleaning and disinfection before and after arterial blood drawing.
WO2012130862A1 Selection of hcv treatment The present invention is based on the discovery of an association between the SNP genotype at the rs12979860 locus in the IL28B gene promoter and the probability of achieving a SVR in HC V-infected patients that are given a triple therapy treatment that contains peginterferon alfa-2a, ribavirin, and a HCV NS5B polymerase inhibitor.
US7750041 Using antihyperplastic agent; diffusion through capillaries; imaging veins, arteries; side effect reduction; antitumor agents The invention relates to a preparation for restenosis prevention. The preparations for restenosis prevention known as yet do not reach sufficient active agent concentrations in the affected sections of the vascular walls as higher doses cause undesirable side effects. The present invention is a preparation to which at least one antihyperplastic agent is added that has a distribution ratio between butanol and water ≧0.5. The lipophilic active agent is absorbed by the vascular wall fast and in sufficient quantity. The preparation may be a liquid that can pass through capillaries and may contain a contrast agent so that the active agent is transferred into the vascular wall without any additional effort while the usually required contrast radiograms are taken. The preparation may also be applied to a catheter.
WO2008055945A1 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)OH and -C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)OH and -C(O)O- alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and -C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, -C(O)OH and -C(O)O-alkyl; aryl; heteroaryl; -C(O)R5; R4 and R5 independently represent alkyl, aryl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl and -alkylheterocyclyl, with the proviso that, when R1 is imidazolyl, -carbocyclyl-imidazolyl, -alkenyl-imidazolyl or -alkyl-imidazolyl, then R3 may not be -C(O)R5.
CA2369979C 4,5-diaryl-3(2h)-furanone derivatives as cyclooxygenase-2 inhibitors The present invention provides a novel class of 4,5-diaryl-3(2H)-furanone derivatives, which inhibit strongly and selectively COX-2 over COX-1. They are useful to treat inflammation, inflammation-associated disorders, and COX-2 mediated diseases.
CN1615904A Process for preparing white arsenic nano particles The preparation process of nano white arsenic particle mixing As2O3 and hydrochloric acid in ratio of 1 mg to 0.02-0.2 ml and stirring magnetically for dissolving; adding ethanol in the amount of 5-10 times hydrochloric acid volume through stirring for another 10-20 min, ultrasonic treatment at 50-60 deg.c for 10-20 min, adding distilled water in the amount of 4-5 times ethanol through stirring for another 10-20 min, packing and microporous filtering to obtain abacterial nanometer white arsenic particle for treating tumor. The nano white arsenic particle in liquid looks as colorless liquid and under microscope, well dispersed circular or elliptic particles of 80 nm and 40 nm size may be seen.
CN102772369A Docetaxel long-circulating naonparticle preparation and preparation method thereof The invention discloses a docetaxel long-circulating naonparticle which comprises docetaxel, copolymer, cosolvent and water for injection. The invention also discloses a preparation method and performance study of the docetaxel long-circulating naonparticles. A water phase containing the cosolvent is dropped into an oil phase containing the docetaxel and copolymer by a reverse solvent dropping process to obtain the naonparticle preparation having the advantages of uniform particle size, high coating ratio and high stability, of which the average particle size is smaller than 200nm.
CN103153279A Skin compositions and methods of use thereof Provided are body corrective cosmetic formulations and methods of use thereof.
WO2010089259A3 Sustained release composition containing quetiapine The present invention is directed to a sustained release pharmaceutical composition containing quetiapine, a pharmaceutically acceptable salt or a derivative thereof, which allows a once-a-day administration of said sustained release pharmaceutical composition to a patient in need thereof. The present invention is further directed to the use of this composition for the treatment of schizophrenia and acute manic episodes associated with bipolar I disorder, and to a process for preparing the pharmaceutical composition.
WO2013135192A1 Novel use of patchoulol A use of patchoulol in preparing antibiotic medicaments, healthcare food products, food products, cosmetics, disinfectants, or daily supplies. The patchoulol is effective against methicillin-resistant bacteria, and can serve as an active ingredient, with excipients or auxiliary ingredients added, in preparing the medicaments, healthcare food products, food products, cosmetics, disinfectant, or daily supplies that are provided with antibacterial effects.
US20110003767 Inhibitors of Acetyl-CoA Carboxylase for Treatment of Neuronal Hypometabolism This invention relates to methods of using inhibitors of the enzyme acetyl-CoA carboxylase (ACC) for the treatment, prevention, inhibition or alleviation of diseases associated with neuronal hypometabolism and/or loss of cognitive function caused by reduced neuronal metabolism such as, for example, Age Associated Memory Impairment (AAMI), Mild Cognitive Impairment (MCI), Alzheimer's disease, Parkinson's disease, Friedreich's Ataxia (FRDA), GLUT1-deficient Epilepsy, Leprechaunism and Rabson-Mendenhall Syndrome, Coronary Arterial Bypass Graft (CABG) dementia, anesthesia induced memory loss, Huntington's disease and many others.
US20080269351 Alkylated hydroxyaromatic compound substantially free of endocrine disruptive chemicals and method of making the same An alkylated hydroxyaromatic compound prepared by reacting at least one hydroxyaromatic compound with a branched olefinic oligomer having from about 20 to about 80 carbon atoms in the presence of a acid catalyst. The alkylated hydroxyaromatic compound has been determined to be substantially free of endocrine disruptive chemicals when the effects were quantified on pubertal development and thyroid function in the intact juvenile female rat.
CN103751181A Application of compound to medicines for treating ischemic brain injury The invention discloses application of a compound Mollolide A to prepare medicines for treating ischemic brain injury, and belongs to the technical field of medicine new application. Mollolide A has treatment effect on ischemic brain injury and has good development application prospect, the application is disclosed for the first time, and Mollolide A has strong treatment activity on ischemic brain injury, so that prominent substantive features and notable progress are possessed.
WO2007057742A3 Novel piperazinone derivatives Compounds, compositions, medicinal compounds, psychotherapeutic agents, and pharmaceutical compositions relating to the formula I, and pharmaceutical salts thereof, wherein R1, R2, R3, Rn, each X, W1, W2, Y1 and Y2 are defined in the specification. Methods of preparing the compounds, compositions, medicinal compounds, psychotherapeutic agents, and pharmaceutical compositions thereof. Methods of treating various disorders and diseases utilizing the compounds, compositions, medicinal compounds, psychotherapeutic agents, and pharmaceutical compositions of the present invention.
US20080064742 2,2-Difluoro-4-(4-hydroxy-phenyl)-6-methoxymethyl-1,2,3,3a,4,9b-hexahydro-cyclopenta[c]chromen-8-ol and formulations The present invention relates to novel benzopyran ER-β agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-β mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypertension, incontinence, colon cancer, prostate cancer, infertility, depression, leukemia, inflammatory, bowel disease, and arthritis. Formula (I), wherein G is —O—, —S(O)—, —CF2—, —C(O)—, —CR1H— or —CR2(OH)—; R is halo, (C1-C4)alkyl or R2—(CH2)m—; R1 is F, hydroxyl, cyano, trifluoromethyl, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, (C1-C4)alkoxy, (C1-C4)alkycarbonyloxy or benzyl; R2 is trifluoromethyl or (C1-C4)alkyl; R3 is cyano, hydroxyl, (C2-C4)alkenyl, (C1-C4)alkoxy or (C1-C4)alkoxycarbonyl; n is 0, 1 or 2; and m is 0, 1 or 2; and pharmaceutically acceptable salts thereof.
CN1827618A Isoquinoline derivatives and their preparation process and application The invention discloses an isoquinoline derivant. The said derivant, with 9,10-dimethoxy -[1,3] dioxide [4,5-g] isoquinoline [3,2-a] isoquinoline -7-ylidehydrochlorate (I) as its representative, reduces plasma cholesterol level by massively absorbing low density lipoprotein cholesterol and changing them to bile acid in liver. The 9,10-dimethoxy -[1,3] dioxide [4,5-g] isoquinoline [3,2-a] isoquinoline-7-ylidehydrochlorate is a new cholesterol lowering compound which is different in cholesterol lowering mechanism from statins. The 9,10-dimethoxy -[1,3] dioxide [4,5-g] isoquinoline [3,2-a] isoquinoline -7-ylidehydrochlorate and other isoquinoline derivants have an extremely low side toxiceffect, so they are safe natural cholesterol lowering compounds.
CN102349910A Compound medicinal composition for ophthalmology and preparation method thereof The invention relates to a compound medicinal composition for ophthalmology. The compound medicinal composition contains brimoxidine and levobetaxolol, wherein the concentration of the brimoxidine is 0.07-0.33 percent (W/V); and the concentration of the levobetaxolol is 0.25-0.5 percent (W/V). The brimoxidine and the levobetaxolo prepared by the invention can be used for remarkably reducing the intraocular pressure level and is beneficial to treating glaucoma diseases.
CN102309481A Application of compound 4-o-methyl-benzenesulfonyl-2(3H)-benzoxazolone and pharmaceutically acceptable salt thereof in preparing non-steroidal anti-inflammatory and analgesic medicines The invention discloses medicinal usage of the compound 4-o-methyl-benzenesulfonyl-2(3H)-benzoxazolone and pharmaceutically acceptable salts thereof, specifically application of the compound and the pharmaceutically acceptable salts thereof in preparing non-steroidal anti-inflammatory and analgesic medicines. According to analgesic and anti-inflammatory tests on mice, after normal administration, the mice have obviously enhanced ability in fighting pain; compared to similar medicines, the compound and the pharmaceutically acceptable salts thereof have a more obvious analgesic effect, have a good inhibition effect on inflammation reactions of animals caused by various factors, and have hypotoxicity according to results of toxicity tests. In a word, the compound 4-o-methyl-benzenesulfonyl-2(3H)-benzoxazolone and the pharmaceutically acceptable salts thereof have the characteristics of good anti-inflammatory and analgesic activity and hypotoxicity, can be industrially synthesized, are cheap, and can be used individually or jointly with other pharmaceutically acceptable pharmaceutic adjuvants to prepare non-steroidal anti-inflammatory and analgesic medicines, thereby providing a novel means and method for clinical treatment of diseases caused by inflammatory pains and opening up a new direction for clinical administration.
US20110042247 Formulations of azacitidine and its derivatives The present invention relates to pharmaceutical formulations comprising azacitidine or its pharmaceutically acceptable salts, including processes for preparing the formulations comprising azacitidine, or salts thereof, and methods of using the formulations for treating various cancer disorders in mammals.
CN102641285A Compound omeprazole capsule and preparation method thereof The invention relates to a compound omeprazole capsule and a preparation method thereof. The capsule consists of omeprazole, sodium bicarbonate and pharmaceutically acceptable officinal carrier, the pH value of the stomach environment can be increased, and the pH value can be maintained for a certain time due to the sodium bicarbonate, so that the omeprazole which is unstable when meets acid is absorbed for taking effect quickly before being damaged by gastric acid. The compound omeprazole capsule is characterized in that the granularity of one of the main medicine compositions, the omeprazole, is controlled to be in a certain range, so that the prepared preparation, namely omeprazole, can be dissolved and absorbed rapidly in the stomach environment and rapidly and quickly plays the role of inhibiting the gastric acid secretion so as to achieve the ideal curative effects.
WO2012011548A1 Nitrogen-containing heterocyclic derivative The present invention provides a nitrogen-containing heterocyclic derivative which has ASK1-inhibitory activity and is useful as a prophylactic and/or therapeutic agent for ALS and so on, or a pharmaceutically acceptable salt thereof. The present invention provides a compound selected from among compound (1), compound (2), compound (3), compound (4), compound (6), compound (7) and compound (8), or a pharmaceutically acceptable salt thereof.
CA2771679A1 4-alkoxy-n- (2-hydroxycarbamoyl-2-piperidinyl-ethyl) -benzamide compounds as selective tace-inhibitors for the treatment of inflammatory diseases The present invention relates to novel benzene- carboxamide compounds having a structure that corresponds to the general formula (I) below: and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.
WO2011019060A1 Hedgehog signal inhibitor Provided are a hedgehog signal inhibitor and the like that contain, as an active ingredient, either a condensed heterocyclic derivative represented by general formula (I) or a pharmacologically permitted salt thereof. In formula (I), R1 represents a hydrogen atom or the like; R3 represents a lower alkyl or the like that may have a substituent; A represents a cycloalkyl or the like that may have a substituent; B represents a five- or six-membered nonaromatic carbon ring or the like that goes together with the -C=C- of the neighboring pyrrole ring and may have a substituent; L1 represents formula (i) or the like; L2 represents formula (iv) (in which R4 represents a hydrogen atom or the like), formula (v), or the like; and M represents formula (x) (in which R2 represents a hydrogen atom or the like; if L2 represents formula (v) or the like then Q does not exist; and if L2 represents formula (iv) then Q either does not exist or represents an oxygen atom) or the like.
CN103690504A Method for preparing rosuvastatin calcium tablet solid dispersion The invention relates to a method for preparing a rosuvastatin calcium tablet solid dispersion. The method comprises the following steps: dissolving rosuvastatin calcium and a water-soluble polymer in a solvent; spraying the mixture in excipient by adopting a spray drying method; adding a pH regulating agent, a disintegrating agent, a stabilizing agent and lubricant, and tabletting. The solid dispersion can be used for remarkably improving the dissolution and stability of rosuvastatin calcium tablets.
US7662807 Sulphonated meso-tetraphenyl chlorins The present invention provides photosensitizing agents obtained by reducing a single double bond in the porphyrin macrocycle of a sulphonated meso-tetraphenylporphyrin, preferably a disulphonated meso-tetraphenylporphyrin such as TPPS2a. The resulting sulphonated meso-tetraphenyl chlorins include compounds of formula (I) (wherein X is —SO3H; n, p, q and r are each independently 0 or 1; and the sum of n, p, q and r is an integer from 1 to 4, preferably at least 2, e.g. 2 or 4) isomers and isomer mixtures thereof. The compounds of the invention and their pharmaceutically acceptable salts find particular use as photosensitizing agents in the photochemical internalization of molecules and in photodynamic therapy.
US20100330114 Use of SIRT1 Activators or Inhibitors to Modulate an Immune Response The present disclosure provides a method of increasing an immune response in an individual, the method involving administering to an individual in need thereof an inhibitor of SIRT1. The present disclosure provides a method of reducing an immune response, e.g., to treat chronic immune hyperactivity, the method generally involving administering to an individual in need thereof an activator of SIRT1. The present disclosure provides a method of modulating activation and differentiation of CD4+T cells.
CN101810568A Injection containing ibuprofen and preparation method thereof The invention provides an injection containing ibuprofen and a preparation method thereof. The injection has the advantages of good stability, high safety and good treatment effect. The injection contains ibuprofen and arginine, wherein the molar ratio of the arginine to the ibuprofen is larger than or equal to 1 to 1.
WO2007039264A1 Pyrazolo [1, 5 -alpha] pyrimidinyl derivatives useful as corticotropin-releasing factor (crf) receptor antagonists The present invention generally relates to the polymorph Form 2 of [3-(4-methoxy-2-methyl-phenyl)-2,5-dimethyl-pyrazolo[1,5-a]pyrimidin-7-yl]-[(S)-1-(3-methyl-[1,2,4]oxadiazol-5-yl)-propyl]-amine. The present invention also relates to pharmaceutical compositions comprising the same and methods of using the same.
CN102363618A Novel inhibitor of epidermal growth factor receptor (EGFR) and application thereof The invention relates to a novel inhibitor of an EGFR and an application thereof. The general formula of the EGFR inhibitor is represented by a formula shown in the specification. In the formula, L is a C1-4 lower alkyl group, a C1-4 lower alkyloxy group, a C1-4 lower alkylamino group, O, OR4, S, SR4, NH or NR4, wherein R4 is a C1-4 lower alkyl group, a C1-4 lower alkyloxy group, or a C1-4 lower monoalkylamino group; R1 is a phenyl group, a substituted phenyl group, a substituted five-nine-membered aromatic cycle, a substituted five-nine-membered aromatic heterocycle or a substituted aromatic bicycle; R2 is hydrogen, a C1-9 alkyl group, a C1-9 alkyloxy group, OH, NH2, NO2, SH, or NR5R6, wherein R5R6 is hydrogen, a C1-9 alkyl group, a C1-9 alkyloxy group or a C1-9 monoalkylamino group, a three-nine-membered substituted aliphatic cycle, an aliphatic heterocycle, a substituted aromatic cycle, a substituted aromatic heterocycle, or a three-nine-membred bicycle; and R3 is halogen, H, SH, OH or NO2. The virtual screening of a computer, EGFR kinase activity inhibition experiments, and cancer cell inhibition experiments confirm that compounds of above formula are the EGFR inhibitor and have good curative effects and prevention effects on cancers related with the EGFR.
US20110263650 Tubulysin D Analogues The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The essential features for the potent cytotoxicity of tubulysin D have been established for the first time by the synthesis and evaluation of a series of analogues. By identifying functionality that surprisingly is not necessary for activity, highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D.
CN101693035A Medicinal preparation with inhibiting effect on tumor metastasis The invention relates to a medicinal preparation with inhibiting effect on tumor metastasis, which contains steroidal saponin extractives. The effective active components of the medicinal preparation comprise the following eight steroidal saponin general extractives which are eight steroid saponins: steroidal saponin I, steroidal saponin II, dioscin, gracillin, steroidal saponin H, steroidal saponin VII, saponin A (pennogenin-3-O-alpha-L-isodulcitol-yl(1-4)-[alpha-L-isodulcitol-yl(1-2)]-alpha-L-isodulcitol-yl(1-2)-beta-D-heteroside) and saponin B (pennogenin-3-O-alpha-L-isodulcitol-yl(1-4)-[alpha-L-isodulcitol-yl(1-2)]-alpha-L-isodulcitol-yl(1-3)-beta-D-heteroside), and the effective active components of the medicinal preparation also comprise medical dressings. The weight content of the eight steroidal saponin general extractives is 5%-30%, and the weight content of the medical dressings is 70%-95%. The invention is a medicinal preparation with less toxic and side effects and inhibiting effect on tumor metastasis.
WO2012078667A2 Compositions and methods relating to proliferative diseases Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described, herein.
US7361373 Carbonized pine cone for treating burns; non-scarring; reduced side effects The present invention relates to an antipyrotic having compositions excellent for treating burn and a normally used carrier in a fixed ratio, and a method of manufacturing the same. The antipyrotic of the present invention has, as its main composition, a carbonized pine cone that is yielded by completely combusting selected pine cones put in a sealed container after washing and drying at a temperature of 100 to 300° C. and has, as an additive, a normally used carrier. As described in detail, the present invention provides provide a cream or ointment type of antipyrotic that can easily treat with excellent treating power serious burn more than the second degree burn as well as slight burn that does not require special treatment by medical specialist. Their treatment ability is excellent and they can shorten the treatment period considerably and leave almost no scars on the skin after complete healing. They are made of plant formulations and thus show almost no side effects to the human body. In the prior treatment of using gauze, the patients complain about pain caused as the gauze and the scab are exfoliated together, when the gauze is removed from the affected region after a certain period. However, the antipyrotic of the present invention can be applied to the affected region softly without causing pains and thus are convenient to use.
CN102920693A Longan flower extract, application of longan flower extract in immunoloregulation, and longan flower extract preparation method The present invention relates to a medical composition for immunoloregulation, wherein the medical composition comprises an effective amount of a separated or purified longan flower extract for immunoloregulation and a pharmaceutically acceptable carrier, the longan flower extract can inhibit human T lymphocyte activation proliferation caused by anti-CD3/CD28 antibody (Ab), IL-2, IFN-gamma and TNF-alpha protein generation in human T lymphocytes caused by anti-CD3/CD28 Ab, IL-2, IFN-gamma and TNF-alpha gene expression in human T lymphocytes caused by anti-CD3/CD28 Ab, and PKC theta and NF-kappaB activation in human lymphocytes caused by anti-CD3/CD28 Ab.
EP1301475B1 Aryl sulfonamides as serotonin antagonist for the treatment of obesity The invention provides a method of treatment or prophylaxis of obesity, comprising administering to a patient in need of such treatment a therapeutically effective amount of an aryl sulfonamide compound of formula (I) or formula (II) wherein the substituents are as described in the specification in which E is -SO2NH- or -NHSO2.
US20110166091 Compositions Containing Piperacillin and Tazobactam Useful for Injection An aminocarboxylic acid chelating agent, preferably EDTA, or a salt thereof has been found to be useful for inhibiting particulate formation in piperacillin/tazobactam parenteral combinations. The composition may also contain a buffer, preferably citrate, and optionally an aminoglycoside. The product may be in the form of a frozen composition that can be thawed for use. The product may also be in the form of a cryodesiccated powder that can be reconstituted by addition of an aqueous vehicle to reform a solution.
US20100305162 Methods for the Synthesis of Pyridoxamine The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): and salts thereof. The invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.
US20090081294 Sustained release dosage form for lubricating an oral cavity Aspects of the invention include a sustained release dosage form that can be administered to an oral cavity, e.g., the mouth. In certain embodiments, the sustained release dosage form is formulated as a lozenge or gum that may be administered to an oral cavity for the purpose of providing lubrication therein. In certain embodiments, the sustained release dosage form not only provides lubrication to a mucosal surface of an oral cavity, but also provides for the sustained release of a flavoring and/or beneficial agent. Accordingly, in certain embodiments, the sustained release dosage form includes a water-insoluble polymer, e.g., ethylcellulose, an essential oil component, and an effective amount of a film forming binder, e.g., xanthan gum. In certain embodiments, the effective amount of the film forming binder and the type of film forming binder are selected so as to provide the sustained release dosage with the capability of lubricating one or more mucosal surfaces within an oral cavity when the dosage form is positioned therein. In certain embodiments, the sustained release dosage form is formulated in a manner sufficient to form a matrix that includes the various components of the sustained release dosage form, such that when positioned in an oral cavity the matrix slowly dissolves and thereby lubricates the oral cavity and/or delivers a flavoring and/or beneficial agent thereto. Methods of formulating such dosage forms and administering them to an oral cavity for the treatment of an adverse condition are also provided.
US20100152173 Tablet Having Improved Stability With At Least Two Actives The present invention relates to a tablet comprising at least a first and second active, the first active being in the form of a non-aqueous granulate, the second active ingredient being in the form of melt extrudated granules or a granulate (aqueous or non-aqueous). The first and second active forms are blended together. The present invention is further directed to a method of producing said tablet.
WO2009004322A2 Derivatives of nystatin and their use as antifungal agents The present invention provides a compound of formula (I') which is a nystatin derivative having an additional double bond present between C28 and C29 and which is further modified relative to nystatin at one or more of positions C5, C7, C9, C1O, C11, C16 or at the amino group of mycosamine. These compounds are used as anti- fungal agents.
US20050085457 Therapeutic quinolone compounds with 5-ht-antagonistic properties Provided herein is a compound having the formula (I) (R2 is typically a tertiary nitrogen atom, being either alkyl-substituted or member of q heterocyclic ring; R7 is typically a monocyclic or bicyclic aromatic ring or a heterocyclic ring) wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.
US20080248553 Recombinant food-grade microorganism for use as bioreactor in production of monoglutamyl folate The invention provides a process of producing bio-available folate, i.e., folic acid having an increased proportion of monoglutamyl folate and a decreased proportion of polyglutamyl folate, by culturing food-grade microorganisms containing an active heterologous or homologous polyglutamyl hydrolase activity or containing increased activities of folate biosynthesis enzymes. The genes encoding the polyglutamyl hydrolase and the folate biosynthesis enzymes may be of various origin, e.g. from rodents or other mammals including man. Also provided is a foodstuff, especially a dairy product containing such monoglutamyl folate-producing microorganisms.
WO2007127212A3 Anti-viral agents that activate rnase l RNase L Activators and methods of using the same are disclosed herein.
WO2010022051A3 Disruptors of early/recycling endosomes A delivery system for introducing a cargo molecule into cytosol of a living cell can include: a first membrane binding element linked to an endosomal compartment disrupting element through a first linker having one or more anionic moieties; and a second membrane binding element linked to an exogenous cargo molecule through a second linker having one or more anionic moieties, the second linker having a region that is selectively cleavable, wherein the first and second membrane binding elements both induce endocytosis into an early/recycling endosome and the endosomal compartment disrupting element destabilizes the early/recycling endosome such that the exogenous cargo molecule is released from the second membrane binding element and into the cytosol of the living cell.
EP2382975A2 Neurogenesis by modulating angiotensin The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes compositions and methods based on modulating angiotensin activity to stimulate or activate the formation of new nerve cells.
EP1844052A1 Thieno[2,3-d]pyrimidine compounds as inhibitors of adp-mediated platelets aggregation Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I): wherein A1, A2, A3, A4, A5, A6, A7, A8, X4, X6, R2, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
CN101849971A Soft capsule containing coenzyme Q10 and preparation method and application thereof The invention discloses a Yixingrui Brand soft capsule containing coenzyme Q10 which can improve immunity and fight against cancers, and a preparation method and application thereof. The preparation method comprises the following steps: using 45-55g of raw medicine containing coenzyme Q10 with content more than or equal to 99 percent as an effective ingredient, using 100-300g of perilla herb oil as solvent, preparing the effective ingredient and the solvent into contents at 40-50 DEG C, proportioning 200-300g of gelatin, 100-250g of glycerin, 250-400g of purified water, 0.8-1.2g of pigment and 1-1.2g of pulpy antholeucin to prepare capsule material, adopting sol to prepare the contents and pressing pellets, conducting processes such as drying, pellet picking and the like of a soft capsule preparation technology, and pressing the material medicine into 1000 Yixingrui Brand soft capsules at 50-55 DEG C through a soft capsule pressing technology. The invention is characterized in that the physical efficacy of the coenzyme Q10 is adopted, solvent, vitamin and minerals with collaborative function are screened and the raw medicine is pressed into pellets by adopting the matured Yixingrui Brand soft capsule preparation technology. According to stability tests, evaluative animal safety tests, hygienic tests and efficacy tests, the invention has the advantages of stable form and efficacy ingredients, no toxic and side effects, strong immunologic function, novel anticancer indication effect and promising application prospect.
US20110165250 Compositions and methods for treatment of neoplastic disease The present invention is concerned with immunostimulant compositions, in particular compositions comprising microparticulate form of murmyl dipeptide, and their use in the treatment of neoplastic disease.
US20080312311 Crystalline forms of 3-(2R-tetrahydrofuryl-methyl)-2-thioxanthine The present invention relates to novel crystalline forms of 3-(2R-tetrahydrofuryl-methyl)-2-thioxanthine. Further the present invention also relates to compositions comprising them and their use in therapy.
CN103385876A Frovatriptan medicine composition and preparation method thereof The invention discloses a medicine composition with which frovatriptan succinate can maintain stable. The composition comprises: a, an active component frovatriptan succinate; and b, other common solid preparation auxiliary materials. The other solid preparation forming auxiliary materials are two or more selected from lactose, starch, hydroxypropyl methyl cellulose, povidone copolymer, high-substituted hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, cross-linked povidone, magnesium stearate, talcum powder, and the like. The invention also discloses a preparation method of the medicine composition.
US20090062199 Nogo Receptor Polypeptides and Polypeptide Fragments and Uses Thereof Nogo receptor 1 (NgR1) is a leucine rich repeat protein that forms part of a signaling complex that modulates axon regeneration. Previous studies have shown that the entire LRR region of Nogo receptor-1, including the C-terminal cap of LRR, LRRCT, is needed for ligand binding, and that the adjacent CT stalk of the Nogo receptor-1 contributes to interaction with its co-receptors. The present invention is directed to the use of certain Nogo receptor-1 and Nogo receptor-2 polypeptides and polypeptide fragments for promoting neurite outgrowth, neuronal survival, and axonal regeneration in CNS neurons. The invention features molecules and methods useful for inhibiting neurite outgrowth inhibition, promoting neuronal survival, and/or promoting axonal regeneration in CNS neurons.
CN1814236A Qishiwei Turguoise pills The invention belongs to the technicl field of Zang medicine, especially relating to a seventy-drug Zang medicine of Songshi pill, characterized by that it is prepared of seventy medicinal materials such as Turquoise, Yanjinggao, Pearl, Largeleaf Gentian Rootú¼Haitum Violaceumú¼Moschus, C. sibirica var. impatiens (Pall.) Regelú¼Nutmeg Seedú¼Pokeberry Rootú¼Dracocephalum tanguticum Maximú¼Herba Lagotisú¼Yinhuiú¼A. pulchellum Hand. -Mazzú¼ Common Bombax Flowerú¼ Cinnabarú¼Herba Swertia chirayitaeú¼Pomegranate seedú¼iron powderú¼Herba Aconiti tanguticiú¼Lignum Santali Albi Santalum album Lú¼Bezoarú¼Semen Herrpetospermiú¼Cassia obtusifolia Lú¼Parmelia saxatilis Achú¼and Kongquelintan by crushing into fine powders, screening, unformly mixing, and making pills with water. It has functions of comforting liver and benefiting gallbladder, and removing blood stasis and stopping pain, applied to curing the diseases such as liver depression and Qi obstruction, swelling pain on sides of the chest caused by damp, heat, and stasis, and inappetence.
CN101209256A Polydatin medicinal composition containing polyvinyl pyrrolidone The invention relates to a high-concentration polydatin drug composition containing polyvinylpyrrolidone, and contains polydatin and solubilizer polyvinylpyrrolidone; the polyvinylpyrrolidone is PVP K15 or PVP K30, the polydatin is in the water solution or physiological saline of polyvinylpyrrolidone (PVP) K15 or K30, and the solubility can achieve the specification of the conventional injection preparation.
US20050042175 Combined doses of formoterol and budesonide The present invention discloses pharmaceutical dry powder combined doses for administration by inhalation of metered dry powder combined doses of finely divided dry medication doses. Formoterol and budesonide are selected medicaments for forming the combined doses. Metered dry powder medicinal combined doses comprising separately metered deposits of medicinally effective quantities of each of the selected medicaments are prepared, in which the sum of the metered deposits constitutes the metered quantities of powder of the combined doses and the medicinal combined doses are introduced into an adapted inhaler device for a generally simultaneous or sequential prolonged delivery of the medicinal combined doses during the course of a single inhalation by a user, such that each one of the administered medicinal combined doses is composed of a high proportion of de-aggregated fine particles of the selected medicament or medicaments and directed to a selected location in the lungs of a user.
EP1844782A1 Use of 4,9-anhydro-tetrodotoxin for the treatment of diseases related to the voltage-gated sodium channel subunit Nav1.6 The present invention refers to the use of 4,9-anhydro-tetrodotoxin for the treatment of diseases related to the voltage-gated sodium channel a subunit Nav1.6.
US7288262 Composition comprising a cyclohexane-based compound, compound and use of said compound to structure a composition Compositions, in particular cosmetic compositions, comprising a cyclohexane-based compound defined by formula (I): wherein: R, which may be identical or different, are each chosen from hydrogen atoms and linear and branched, saturated hydrocarbons comprising 1 to 6 carbon atoms; Y, which may be identical or different, are each chosen from —CO—S—R′ groups, —CO—NHR′ groups, NH—COR′ groups and —S—COR′ groups, wherein R′, which may be identical or different, are each chosen from hydrogen atoms, aryl groups, optionally substituted with at least one hydrocarbon comprising 1 to 22 carbon atoms, wherein said hydrocarbon is chosen from linear and branched, saturated and unsaturated hydrocarbons, and linear, branched and cyclic, saturated and unsaturated hydrocarbons comprising 1 to 22 carbon atoms, wherein said hydrocarbons may optionally be substituted with at least one group chosen from aryl groups, ester groups, amide groups and urethane groups; wherein said hydrocarbons may optionally comprise at least one hetero atom chosen from O, S and N; and wherein said hydrocarbons may optionally be substituted with at least one entity chosen from fluorine atoms and hydroxyl groups; with the proviso that at least one of said R′ comprises at least one unsaturated hydrocarbon. Compounds of formula (I) and their use for structuring a composition, in particular a cosmetic composition.
CN102784277A Plant antihypertensive thrombolytic tablet A plant antihypertensive thrombolytic tablet is the latest product invented at present for special treatment of hypertension and thrombolysis. The tablet is prepared by people's daily consumption of vegetable concentrated juice, and trace element chromium. The tablet has a novel and unique formula, is easy and convenient in a taking method, and is good in effect. People who take the tablets can realize the purpose of reducing blood pressure by eating and drinking.
US6936623 Pyrano[2,3-C]imidazo[-1,2-A]pyridine derivatives for the treatment of gastrointestinal disorders Compounds of the formula (I), in which the substituents have the meanings mentioned in the description, are suitable for the prevention and treatment of gastrointestinal diseases.
EP0928184B1 Anti-caries oral compositions The present invention relates to oral compositions containing anti-caries agents distributed in an oral vehicle. In particular, the present invention provides oral compositions containing calcium, arginine and a cariostatic anion distributed in an oral vehicle. A method for preparing oral compositions containing anti-caries agents is also provided by the present invention. A method of reducing dental caries is described which comprises delivering a therapeutically effective amount of an oral composition containing calcium, arginine and a cariostatic anion into the oral cavity.
CN101575333A Quinazoline derivatives and medical application thereof The invention discloses a quinazoline derivatives of structural formula (I). The quinazoline derivatives can be used for preparing medicaments for diseases correlative to angiogenesis, particularly, can be used for preparing medicaments for treating tumor, age-related macular degeneration or chronic inflammation.
EP2494968A1 Compound, in particular dermatological ointment with Olea Europaea Fruit Oil and Silver Composition, preferably dermatological ointment comprises Olea europaea fruit oil, urea, silver, and octyldodecanol, Echium plantagineum seed oil, Cardiospermum halicacabumleaf extract, unsaponifiable Helianthus annuus seed oil and tocopherol. - ACTIVITY : Dermatological. - MECHANISM OF ACTION : None given.
US20120027878 Natural lycopene concentrate and method for production thereof Natural lycopene concentrate obtained from a plant structure after alkalinization, solid-liquid separation, acidification and a second solid-liquid separation. The concentrate obtained is highly bioavailable and water-soluble at room temperature.
EP1311260B1 Lipase inhibitors to treat dyspepsia The present invention refers to the use of lipase inhibitors, e.g. orlistat, for the manufacture of medicaments for treating, reducing or preventing functional dyspepsia, e.g. intensity of stomach fullness, nausea, bloating after ingestion of small or larger meal, especially of fat containing or fat rich meals, and the medicaments thus manufactured.
EP1731042A1 Feed additive for laying hens and feed containing the additive A feed additive for laying hens comprising lactobionic acid or a lactobionic acid salt and a feed characterized by containing a feed additive for laying hens comprising lactobionic acid or a lactobionic acid salt and a feed. Namely, a feed additive for laying hens, which is excellent in effect of reinforcing eggshells, shows a particularly remarkable effect of improving eggshell qualities in the second half of the laying period, relieves stress caused by forced molting, cage transfer and so on and can inhibit lowering in the egg-laying rate.
CA2741069A1 Inhibitors of mitosis for increasing apoptosis in therapy An inhibitor of mitosis for administration to a patient having pathogenic cells in a state of mitosis inhibitor-in-duced mitotic arrest, for increasing apoptosis of the cells.
WO2005014001A9 Use of 2h- [1, 3] - oxazino [3, 2-a] indole derivatives for the treatment of neuropathic pain Use of a compound of formula (I), wherein R is H, a linear or branched alkyl chain having from 1 to 12 carbon atoms or an arylalkyl group, and of the acid addition salts thereof with pharmaceutically acceptable organic or inorganic acids, to prepare a pharmaceutical composition active in the treatment of neuropathic pain.
CN101468050B External use medicament for treating viral keratitis and preparation method thereof The invention discloses an external medicine for treating keratitis, especially for treating viral keratitis, comprising borneol, pearls, natural indigo, musk, bear bile, bezoar, calamine, cuttlebone as raw materials, processed by grinding into powder mixture, with obvious drug effect and short administration time, low recurrence rate.
US20120157510 Controlling The Potential Of Primate Neural Stem Cells By Regulating Pax6 A transcription factor both necessary and sufficient for human neuroectoderm specification, Pax6, as well as applications thereof, is disclosed.
WO2005087762A1 Novel indole derivative for alkylating specific base sequence of dna and alkylating agent and drug each comprising the same A novel pyrrole-imidazole polyamide type compound for alkylating a specific base sequence of a DNA. It can be synthesized through fewer reaction steps than conventional hybrid molecules and combines high reactivity in DNA alkylation with the ability to recognize a sequence. Also provided are an alkylating agent and a molecule functioning as a drug which each comprises the compound. The novel compound is an indole derivative represented by the following general formula (1) wherein R1 represents a functional group alkylating a DNA; R2 represents hydrogen, alkyl, or acyl; and X represents either a divalent group consisting of one of the structural units represented by the following formulae (2) (wherein m is an integer of 0 to 10) or a divalent group composed of two or more identical or different structural units selected among those structural units, provided that the structural unit present at the R2-side end of the structural units may be any of the following formulae (3) (wherein k is an integer of 0 to 10).
CN101028265A Black and white medicinal composition for improving sleep and adjusting sleep-rhythm functions A composite black-white medicine for improving sleep quality and regulating sleep rhythm is composed of a black component taken at night and containing diphenhydramine and VB6 and a white component taken in the day and containing aspirin and caffeine.
CN103251954A Diabetes treating compound medicine for reducing side effect of rosiglitazone and preparation method thereof The invention discloses a diabetes treating compound medicine for reducing side effect of rosiglitazone and a preparation method thereof, and belongs to the field of medicine preparation. The compound medicine consists of rosiglitazone and a diuretic medicine, wherein the ratio of rosiglitazone to the diuretic medicine by weight is 1:(0.04-1). The diabetes treating compound medicine is compounded and matched with any one of spirolactone, amiloride, compound amiloride, ergosterol, triamterene, ethacrynic acid, hydroflumethiazide and bumetanide which can better eliminate side effect of rosiglitazone with rosiglitazone so as to form the compound medicine which not only can reduce the side effect of rosiglitazone, but also better treats diabetes.
CN101347477B Medicament composition for treating rheumatoid arthritis The present invention pertains to the field of medicine technology and discloses a medicine combination for curing rheumatoid arthritis. The combination contains the raw materials with the following weight rate: 7,680 to 8,320 portions of Common Andrographis Herd, 576 to 624 portions of scandent schefflera stem and leaf , 4 to 8 portions of menthol and the rest of auxiliary materials; the Common Andrographis Herd of the combination can be replaced by the extract andrographolidume of Common Andrographis Herd and scandent schefflera stem and leaf can be replaced by stem and leaf extract; the weight rate of Common Andrographis Herd extract, scandent schefflera stem and leaf extract and menthol is as follows: 48 to 112 portions of andrographolidume, 40 to 94 portions of scandent schefflera stem and leaf extract, 4 to 8 portions of menthol and the rest of auxiliary materials.
CA2095659C Heteroatoms-containing tricyclic compounds The invention concerns the compounds of formulae (see formula I, II, III) wherein the substituents have various significances. They can be prepared by various methods, e.g. acylation, reduction, alkylation, etc. They are indicated for use as pharmaceuticals, in particular as immunosuppressant, antiproliferative and antiinflammatory agents.
EP1420645B1 Multivesicular emulsion topical delivery systems A topical delivery composition which employs a multivesicular emulsion in combination with a pharmaceutically/pharmacologically active agent is disclosed. The multivesicular emulsion is formed from a quaternary amine salt emulsifier such as behentrimonium methosulfate. The emulsion is multi-lamellar which is a series of concentric spheres or vesiculars of oil and water phase that can be seen microscopically. As a result, the active is time released over a sustained period rather than spike released as is common with most topicals.
CA2860932A1 A pharmaceutical composition comprising stable, amorphous hybrid nanopraticles of at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component The present invention relates to the field of methods for providing pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to compositions comprising stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions and in therapy.
WO2005111078A3 Anti-cea scfv-beta-lactamase contructs (cab molecules) in adept The present invention relates to CAB molecules, ADEPT constructs directed against CEA, and their use in therapy.
CN101513418A Application of 1,11-dyhydroxy-oleanane-28-acid-2,12-diene in preparing medicament for treating skin diseases The invention discloses application of 1,11-dyhydroxy-oleanane-28-acid-2,12-diene in preparing medicament for treating skin diseases, and provides a pharmaceutical composition. The pharmaceutical composition is characterized by comprising the 1,11-dyhydroxy-oleanane-28-acid-2,12-diene (I) which is taken as an active component and one or more medicinal accessories. In the pharmaceutical composition provided by the invention, the medicinal accessories are all administrative accessories which are suitable for the skin or mucosa.
US7064116 GABAA modulating neurosteroids The present invention relates to novel steroid derivatives that ace on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex as well as methods for making the same and their applications to induce anesthesia, in the treatment of stress, anxiety, PMS, PND, and seizures such as those caused by epilepsy, to ameliorate or prevent the attacks of anxiety, muscle tension, and depression common with patients suffering from central nervous system abnormalities. The present invention comprises a compound represented by Formula (I): wherein, R, R1, R2, R3, R4, R5 are defined in the description of the invention. The present invention also includes formulations which consist of one or more of the compounds of Formula (I).
WO2014003154A1 Agent for preventing deterioration in vascular endothelial function or improving vascular endothelial function An NO production-enhancing agent, which comprises citrulline or a salt thereof and serine or a salt thereof as active ingredients; an agent for preventing the deterioration in a vascular endothelial function or improving the vascular endothelial function, which comprises citrulline or a salt thereof and serine or a salt thereof as active ingredients; and a prophylactic or ameliorating agent for conditions associated with the deterioration in a vascular endothelial function, which comprises citrulline or a salt thereof and serine or a salt thereof as active ingredients.
US20070265196 Method of Modulating Pro-Inflammatory and Inflammatory Activity Mediated by C-Reactive Protein The present invention relates generally to a method of modulating the proinflammatory activity of C-reactive protein in endothelial cells. More particularly, the present invention relates to down-regulation of proinflammatory activity of C-reactive protein in vascular endothelial cells. Accordingly, the method of the present invention is useful, inter alia, in the treatment and/or prophylaxis of inflammatory conditions, particularly conditions characterised by proinflammatory activity of C-reactive protein in endothelial cells.
US7119117 Tocopherol enriched compositions and amelioration of inflammatory symptoms The present invention provides non-alpha-tocopherol enriched tocopherol compositions and non-alpha-tocopherol metabolite enriched compositions for use in the reduction of inflammatory markers associated with inflammation such as C-reactive protein.
EP1056724B1 Substituted cycloalkyl-4-oxonicotinic carboxamides; gaba brain receptor ligands Disclosed are compounds of Formula (a) or the pharmaceutically acceptable non-toxic salts thereof wherein: the C ring is a(n) (un)substituted carbocycle; X is hydrogen, hydroxyl or lower alkyl; and W is (un)substituted alkyl, aryl, arylalkyl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
WO2011146589A8 Vitamin e conjugates, and their uses as antioxidants and prodrug delivery vehicles Tocopherol conjugates are disclosed that are useful as antioxidants or as pro-drug delivery vehicles. The conjugates are amphiphilic, and tend to localize at the interface between water domains and lipid domains. A prototype embodiment disclosed is an alpha tocopherol-linker-carnosine conjugate that has been designated VECAR.
WO2013175047A1 Use of a compound of formula (i) to manufacture a medicament for treating gaucher's disease, pharmaceutical composition, a compound of formula (ib) and method for obtaining said compound Use of a compound of formula (I) to manufacture a medicament for treating Gaucher's disease in a human subject, a pharmaceutical composition comprising a compound of formula (I), compounds of formula (Ib) and method for obtaining said compounds.
EP1522542A1 Therapeutic or preventive agent for nausea/vomiting The present invention provides a therapeutic or prophylactic agent for preventing nausea and vomiting. The agent includes a morphinan derivative represented by general formula (I): or a pharmacologically acceptable acid addition salt thereof as an active ingredient, (where R1 represents, for example, a cyclopropylmethyl group, R2 and R3 represent, for example, a hydroxy or methoxy group, R4 and R5 together form, for example, an -O- bond, R6 represents, for example, a hydrogen atom, Q represents a substituted or unsubstituted group represented by, for example, the following formula: where X represents, for example, NH or NMe). The compounds of the present invention can be widely used as medicines against vomiting caused by emetic drugs. In particular, the compounds of the present invention are useful as therapeutic or prophylactic agents for preventing nausea and vomiting caused by µ-agonists represented by morphine.
US7378425 For preventing, treating and/or improving a disease against which a sigma receptor binding action and/or an acetylcholinesterase inhibitory action is efficacious The present invention provides an excellent sigma receptor binding agent and/or acetylcholinesterase inhibitor containing an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound. More specifically, it provides an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: In the formula (I), R1, R2, R3 and R4 are the same as or different from each other.
CN1679578A Fluorouracil injecting emulsion and production thereof An emulsion injection of fluoroplex for treating colon cancer, rectum cancer, stomach cancer, breast cancer and primary liver cancer is proportionally prepared from fluoroplex, plant oil for injection, polyose, emulsifier, isotonic regulator, and the water for injection through dissolving, heating, mixing, emulsifying, cooling and sterilizing.
WO2005105128A1 Methods of producing treated ganoderma lucidum product and processed ganoderma lucidum product It is intended to provide a method of producing a treated Ganoderma lucidum product characterized by treating G. lucidum with water or steam at 150 to 210°C; or a method of producing a processed G. lucidum product characterized by 1) cutting or milling the treated G. lucidum product, and 2) extracting it with an aqueous solvent, optionally followed by 3) further concentrating the extract obtained in the above 2) or drying the same to give a powder. According to these methods, treated G. lucidum products or processed G. lucidum products can be industrially advantageously produced. Because of having an excellent antitumor effect, these treated G. lucidum products and processed G. lucidum products are useful as medicines or foods and drinks.
CN101045059A Anticarcinogen composition carried with both nitrosourea type medicine and guanine analog An anticancer composition in the form of slow-release injection or implant containing the nitrosourea-type medicine and guanine analog (benzyl guanine, butyl guanine, or alkyl guanine) as the active anticancer components is composed of the slow-release microballs containing said active anticancer components and the slow-release auxiliary chosen from p(LAEG-EOP), p(DAPG-EOP), etc, and the solvent which may be ordinary solvent or a special solvent containing suspending aid.
EP1965669B1 Composition comprising oligosaccharides as soluble dietary fibres for use against muscle wasting A composition nutritional containing dietary fibres is useful for the treatment of muscle wasting, if the dietary fibre comprise at least 30 wt. % of galacto-oligosaccharides or other oligosaccharides having mainly anhydropyranose units, and having a chain length of 3-10 units. The composition may further contain other oligo- or polysaccharides, especially polysaccharides having a majority of anhydrofuranose units.
CN101519423A Betulinic acid analogue and preparation method and application thereof The invention relates to the field of antineoplastic medicines and provides a betulinic acid analogue with the structure shown in figure (1) or solvate thereof. The definition of R1, R2, X and n is in the specification. The invention also provides the a preparation method of the betulinic acid analogue with the structure shown in figure (1) or the solvate thereof, and the applications of pharmaceutical compositions containing the betulinic acid analogue or the solvate thereof and medicines using the betulinic acid analogue or the solvate thereof as the effective constituent for preparing antineoplastic medicines for treating pulmonary cancer, prostatic cancer, colon cancer, leukemia, mammary cancer, liver cancer, gastric cancer, pancreatic cancer, malignant neuroglioma, cerebral tumor, and the like.
US20090291150 Method and compositions for treating and preventing seizures by modulating acid-sensing ion channel activity This invention provides novel methods and compositions for treating and preventing seizures by administration of ASIC1a receptor activating compounds. A novel method of assaying ASIC1a receptor activating compounds is included in the present invention. According to the invention applicants have demonstrated that seizure duration, intensity, and progression may be modulated by administration of an ASIC1a receptor activator which acts to increase the endogenous activity of ASIC1a receptors to mediate the effects of low pH in the CNS. The inventors have also found that the ASIC1a receptor activator may prevent such seizures altogether.
WO2007024338A3 3 -ester prodrugs of ethynylestradiol The present invention is a prodrug derivative of ethinyl estradiol according to Formula I: Formula I
CN101143130A Carmustine intravenous emulsion and its preparation method The invention relates to a carmustine combination, which is used for the vein transfusion and is in a stable oil-in-water emulsion. The invention also relates to the method of mixing the carmustine into the oil to form the stable oil-in-water emulsion. The combination includes the carmustine, the oil, the water and a surfactant.
US20100272802 Compositions comprising strontium and uses thereof in the treatment or prevention of gingivitis, periodontitis, periodontitis as a manifestation of systemic diseases, and necrotizing periodontal diseases The present invention relates to the use of a pharmaceutical composition comprising at least one strontium salts for the preparation of a medicament for treatment and prevention of gingivitis, periodontitis (aggressive and chronic), periodontitis as a 5 manifestation of systemic diseases and/or necrotizing periodontal diseases. The composition preferably comprises strontium carbonate, strontium chlorides and/or strontium renalate. Further included may be a vitamin D compound, preferably vitamin D3.
WO2007028905A1 Use of agomelatine in order to obtain medicaments which are intended for the treatment of sleep disorders among depressed patients The invention relates to the use of agomelatine or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide in order to obtain medicaments which are intended for the treatment of sleep disorders among depressed patients.
US20110212905 Crystalline form of 1-(beta-d-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate A novel crystal form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, and having favorable characteristics, is characterized by its x-ray powder diffraction pattern and/or by its infra-red spectrum.
US20110152289 Dimeric derivatives of artemisinin and application in anti-cancer therapy The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I) below: Formula (I) and the pharmaceutically acceptable salts thereof, and also to the preparation method thereof and to the uses thereof, especially in the treatment of cancer.
EP1337558B1 A "bach" g protein coupled receptor polypeptide and polynucleotide encoding this receptor We disclose BACH G-protein coupled receptor (GPCR) polypeptides comprising the amino acid sequence shown in SEQ ID NO.3 or SEQ ID NO: 5, and homologues, variants and derivatives thereof. Nucleic acids capable of encoding BACH polypeptide are also disclosed, in particular, those comprising the nucleic acid sequences shown in SEQ ID No. 1, SEQ ID No.2 or SEQ ID NO: 4 or a mouse BACH genomic sequence (SEQ ID NO: 10).
EP2570123A1 Use of 2,4-dichlorobenzyl alcohol having an anaesthetic effect The present invention relates to the use of 2,4-dichlorobenzyl alcohol for the preparation of a medicament wherein the 2,4-dichlorobenzyl alcohol exhibits an anaesthetic effect.
CN1857726A Medicine composition for treating hypertension complicated with hyperlipemia and cardiac and cerebral vascular diseases The medicine composition for treating hypertension complicated with hyperlipemia and cardiac and cerebral vascular diseases belongs to the field of medicine technology, and aims at raising the comprehensive curative effect. Technologically, the medicine composition consists of levoamlodipine and its medicinal salt, HMG-COA reductase inhibitor and its medicinal salt and medicine carrier, with the content being levoamlodipine 1.25-20 mg and HMG-COA reductase inhibitor 2.5-100 mg. Owing to the adding or synergistic effect of the medicines, the present invention has obviously raised medicinal effect, reduced dosage and obviously lowered side effect.
US20120077801 Chemical Compounds 637 The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.
US7211589 Atisane compounds and use thereof The present invention provides a novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z represents a bivalent organic group and the like of from 2 to 3 carbon atom(s) which may have a substituent; and R3 represents a carboxyl group and the like.
WO2010007794A1 Novel spiro compound, and pharmaceutical preparation comprising the same Disclosed is a novel compound useful as a prophylactic and/or therapeutic agent for diabetes, insulin resistance, diabetic complications, obesity, dyslipidemia, hypertension, fatty liver or metabolic syndrome. Specifically disclosed is a spiro compound represented by general formula (1), a salt of the spiro compound, or a solvate of the spiro compound or the salt.
US8293745 Use of imatinib to treat liver disorders and viral infections The present invention relates to the use of imatinib for treating viral liver diseases and in particular for viral hepatitis. The invention provides the use of imatinib for inhibiting replication, transmission or both of hepatitis viruses. The invention further relates to the use of imatinib for inhibiting replication, transmission or both of other viruses including herpes virus, poxvirus, influenza virus, para influenza virus, respiratory syncytial virus, rhinovirus, yellow fever virus, west nile virus, and encephalitis virus.
CN102178827A Medicine used for treating breast sore The invention relates to a medicine used for treating breast sore that consists of radix angelicae, pollen, rhizoma anemarrhenae, frankincense, spina gleditsiae, Pangolin Scales, Pinellia ternata, Fritillaria thun-bergli, honeysuckle, raw Astragalus mongholicus and Large leaf Tea. Added with 1500ml of water, all ingredients are decocted to 400ml and then added with 50g of raw yellow wine. The medicine is to be taken on an empty stomach in the morning and at night, and can lead to heal the disease after administration of 5-7 dosages. The medicine has the efficacies of clearing heat and removing the toxin, invigorating the circulation of blood and dissipating stagnation, and is quick and fine in effect when used for treating breast sore, with the total effective rate up to 98.1%.
WO2013181322A1 Methods of administering nitric oxide to arterial or arterialized blood The present invention provides methods of administering nitric oxide (NO) to a patient, the method comprising delivering nitric oxide-containing gas directly into arterial or arterialized blood. The methods of the present invention may be used in the treatment or prevention of a variety of diseases and disorders responsive to nitric oxide, including those resulting from ischemia or hypoxia.
CA2796070A1 Androgen induced oxidative stress inhibitors Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of cancer.
WO2009130016A1 Dihydropteridinones as plk inhibitors The present invention provides derivatives of dihydropteridione of formula (I). These compounds are inhibitors of Polo-like kinases (Plks), including compounds that show antiproliferative activity against cells, including against tumor cells, and are useful in the treatment of diseases including cancer.
WO2004078213A9 Composition for target substance introduction and method of target substance introduction A composition for target substance introduction comprising a target substance, such as peptide, peptide hormone, protein, nucleoprotein, nucleic acid, nucleic acid derivative, essential amino acid, essential fatty acid, vitamin or low-molecular drug, or the target substance together with HVJ envelope vector, and a biocompatible composition of mucopolysaccharide, salt thereof, etc. capable of holding them on tissues. The target substance can be held on tissues and further introduced in cells by administration of this composition to tissues.
CN102743550A Medicine composition for accelerating healing after fracture surgery, preparation method and application The invention provides a medicine composition for accelerating healing after a fracture surgery, a preparation method and application. The medicine composition comprises chaff flower root, epimedium herb, walnut kernels, common gendarussa herb, eucommia bark, cistanche, semen psoraleae, caulis spatholobi, pseudo-ginseng, native copper, rhizoma Chuanxiong, motherwort, caulis piperis futokadsurae, radix astragali, Chinese yam, dried orange peel, costus root and acorus gramineus. By the aid of the medicine composition, secretion of growth factors can be promoted, local blood circulation and metabolic level of fracture can be promoted, metabolism is accelerated, and the fracture rapidly heals.
US6946452 Use of N-acetyl-D-glucosamine in the manufacture of pharmaceutical useful for treating motion sickness The present invention has disclosed a use of N-acetyl-D-glucosamine in the manufacture of a medicament for preventing and treating motion sickness, the preparation in which N-acetyl-D-glucosamine is taken as a main active component is able to be used for preventing and treating motion sickness with an effective rate up to more than 90%.
WO2010057856A8 Use of escin for treatment of type iv hypersensitivity reaction The present invention provides the use of escin for the manufacture of a pharmaceutical preparation for the treatment of a Type IV hypersensitivity reaction or symptoms of a Type IV hypersensitivity reaction, such as in contact dermatitis, atopic dermatitis, hypersensitivity pneumonitis, chronic transplant rejection, graft versus host disease, cell mediated autoimmune diseases, Hashimoto's thyroiditis, Sjogren's disease, adrenalitis, polymyositis, or pernicious anemia.
US20070274947 Antisense Oligonucleotides Directed to Ribonucleotide Reductase R1 and Uses Thereof in the Treatment of Cancer The present invention provides antisense oligonucleotides directed to a mammalian ribonucleotide reductase R1 gene and combinations of the antisense oligonucleotides with one or more chemotherapeutic agents for use in the treatment of cancer.
US20110046210 Substituted thiopenecarboxamides as ikk-beta serine-, threonine-protein kinase inhibitors Compounds of formula (IA) or (IB) are IKK inhibitors useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; A is an optionally substituted aryl or heteroaryl of 5-13 ring atoms; Z is a radical of formula R1C(R2)(R3)NH—Y-L1-X1-(CH2)z— wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 independently represent the side chain of a natural or non-natural alpha amino acid but neither of R2 and R3 is hydrogen, or R2 and R3 taken together with the carbon atom to which they are attached form a C3-C7 cycloalkyl ring, and z, Y, L1 and X1 are as defined in the claims.
US20050075351 4-(Azaindol-3-yl)-quinazoline, 4-(azaoxindol-3-yl)-quinazoline, or 4-(diazaindol-3-yl)-quinazoline derivatives as glycogen synthase kinase inhibitors; Alzheimer's, Parkinson's, Huntington's disease; Down syndrome, amyotrophic lateral sclerosis; neurodegenerative and brain disorders; cognition activators The present invention relates to a new use of oxindole derivatives of formula I, as a free base or pharmaceutically acceptable salts thereof, in the manufacture of a medicament for the prevention and/or treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3. Formula (I) wherein R1, R2, R3, ring Z, m and n are as defined as in claim 1. The present invention further relates to a method of prevention and/or treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3, as well as a pharmaceutical composition for said use.
WO2014135245A1 9-(aryl or heteroaryl)-2-(pyrazolyl, pyrrolidinyl or cyclopentyl)aminopurine derivatives as anticancer agents Compounds of the Formula (I) in which X, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
EP2070922A1 Azabicyclo(3.1.0) hexane derivatives useful as modulators of dopamine D3 receptors The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein • G is phenyl and (R1)p is 4-trifluoromethyl; • R2 is hydrogen; • R3 is methyl; • R4 is 4-pyridazinyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.
US20100310515 Latency Associated Protein Construct With Aggrecanase Sensitive Cleavage Site The present provides a fusion protein comprising a latency associated peptide (LAP) and a pharmaceutically active agent in which the LAP and the pharmaceutically active agent are connected by an amino acid sequence comprising an aggrecanase proteolytic cleavage site.
US20110118258 Quinazolin-oxime derivatives as hsp90 inhibitors Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.
EP1722770A1 Use of metformin and orlistat for the treatment of prevention of obesity The present invention relates to the use of metformin and orlistat to treat patients suffering from obesity.
US20110218158 Dna cytosine deaminase inhibitors Cytosine deaminase inhibitors and methods for identifying inhibitors of the anti-retroviral activity of APOBEC3G are described.
US7514443 pyrazolo- and imidazo-pyrimidine derivatives; for anxiety and pain, neurodegenerative disorders; 8-Pyridin-4-yl-4-trifluoromethyl-2-(4-trifluoromethyl-phenyl)-imidazo[1,5-a]pyrimidine The present invention relates to novel pyrazolo- and imidazo-pyrimidine derivatives of formula I wherein A, D, E, L, M, Q, R1, R2 and R3 are as defined hereinabove. The present invention also relates to a process for their preparation, a pharmaceutical composition containing said derivatives and a method of treating or preventing acute or chronic neurological disorder comprising administering to a patient in need of such treatment a pharmaceutical composition comprising a therapeutically effective amount of at least one such derivatives. These disorders include acute and chronic disorders.
US20120214803 Novel Sulfonaminoquinoline Hepcidin Antagonists The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
US20120046218 Glycosaminoglycan-antagonising mcp-i mutants and methods of using same Novel mutants of human monocyte chemoattractant protein 1 (MCP-1) with increased glycosaminoglycan (GAG) binding affinity and knocked-out or reduced GPCR activity compared to wild type MCP-1, and their use for therapeutic treatment of inflammatory diseases.
US20110082098 Novobiocin analogues and treatment of polycystic kidney disease Novobiocin analogues are useful in methods of treating, inhibiting, and/or preventing cyst formation in autosomal dominant polycystic kidney disease (ADPKD) in a subject. The disclosure provides methods of treating ADPKD comprising administering a therapeutically effective amount of a coumarin-3-carboxamide novobiocin analogue. Accordingly, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of mTOR pathway phosphoproteins P-mTOR, P-Akt and P-S6K, or combinations thereof. Further, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of Hsp-90 client proteins CFTR, ErbB2, c-Raf and Cdk4, or combinations thereof.
WO2013044356A1 Pharmaceutical compositions comprising phosphate binder, calcium receptor-active compound and/or active vitamin d The present invention is an oral solid pharmaceutical compositions for the treatment of kidney diseases and mineral bone disorder including a phosphate binder, a calcium receptor-active compound and at least one pharmaceutically acceptable excipient, the invention further including a method for preparing the pharmaceutical compositions including the steps of granulating cinacalcet and/or sevelamer and/or vitamin D by one of a wet and a dry granulation process, each with at least one pharmaceutically acceptable excipient to form cinacalcet granules and/or sevelamer granules and/or vitamin D granules, mixing at least two of the cinacalcet granules, sevelamer granules and vitamin D granules to form a granules mixture and compressing the granules mixture to tablets or encapsulating the granules mixture into capsules or pulverizing the granules mixture into a dispersion powder.
CN103610636A Medicinal composition containing epigallocatechin gallate and application of medicinal composition The invention provides a medicinal composition containing epigallocatechin gallate and an application of the medicinal composition. The composition is prepared by mixing the following raw materials in parts by weight: 0.002-0.2 part of epigallocatechin gallate, 0.09-3 parts of sodium chloride, 0.05-5 parts of citric acid and 90-99.9 parts of ultrapure water or distilled water. The medicinal composition is used for preventing and treating acute radioactivity esophageal injury.
CN101002804A Pure natural preparations used as depressor and hypolipidemic, and preparing method thereof A natural used as both medicine and food for treating hypertension and hyperlipemia is prepared from edible vinegar, egg, honey, crystal sugar and alum. Its preparing process is also disclosed.
CN203564510U Fumigating device for encephalopathy The utility model discloses a fumigating device for encephalopathy. The fumigating device for the encephalopathy comprises a pot body, an upper cover, a steam pipe, a hood and fumigation cylinders. The fumigating device for encephalopathy is characterized in that a power interface is arranged at the bottom of the pot body, a partition is arranged inside the pot body, the upper cover is arranged on the top portion of the pot body, an exhaust pipe is arranged on the top portion of the upper cover, one end of the steam pipe is connected with the exhaust pipe, and the other end of the steam pipe is connected with a multi-channel commutator; four fumigation cylinders are arranged on the hood, the hood comprises a cylinder body I and a hemispheric-shaped cylinder cover I, the hemispheric-shaped cylinder cover I is arranged on the top end of the cylinder body I, each fumigation cylinder comprises a cylinder body II, a hemispheric-shaped cylinder cover II and a fume material cylinder, the hemispheric-shaped cylinder cover II is arranged on the top end of the cylinder body II, an intubation interface is arranged on the middle portion of the outer side of the hemispheric-shaped cylinder cover II, and the cylinder body I is connected with the lower end of the cylinder cover II. The fumigating device for encephalopathy is reasonable in design, has multiple functions, can not only conduct a smoked therapy, but also conduct vaporization, can gather the smoked therapy and the vaporization in one device and is convenient to use.
CN103524456A Selenazole acid compound and selenazole acid salt The invention relates to a selenazole acid compound as shown in the formula I or a pharmaceutically acceptable salt, aquo-complex and solvate, and provides a preparation method of the compound and an application of the compound in preparation of a medicine for treating and preventing hyperuricemia and medicines for treating gout, arthritis or cardiac failure caused by hyperuricemia. The definition of the substituent group of M in the formula I is the same with the definition in the specification.
US6890952 Administering cyclic substituted aminomethyl compounds for the preparation of a drug for the treatment of pain, urinary incotinence, itching, tinnitus aurium or diarrhea in a mammal Cyclic substituted aminomethyl compounds of general formula IA and IB, methods for production thereof, intermediates in said production methods, a medicament containing at least one of said cyclic substituted aminomethyl compounds, the use of said cyclic substituted aminomethyl compounds for the production of a medicament, pharmaceutical compositions containing said compounds, and methods for the treatment of pain, incontinence, pruritis, tinnitus aurium and/or diarrhea using said pharmaceutical compositions.
US20120027814 Polymeric Fibers Having Tissue Reactive Members A method for bonding a polymeric fiber to tissue is provided which includes providing a polymeric fiber having a plurality of tissue reactive members linked to a surface of the fiber via a specific binding pair, and contacting the polymeric fiber to biological tissue, to covalently bond the fiber to the tissue.
CN102918036A 5-amino-3,6-dihydro-1h-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (bace) The present invention relates to novel 5-amino-3,6-dihydro-1H-pyrazin-2-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretaseis involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.
US20110053898 Topical composition comprising vitamin d analogue and corticosteroids A topical pharmaceutical composition comprising therapeutically effective amounts of vitamin D or vitamin D analogues, corticosteroid and a straight chain C6-C28 fatty alcohol.
CN101890070A Wind phlegm fast expelling wine The invention discloses a method for preparing wind phlegm fast expelling wine and is implemented by adopting the following technical proposal. Four pieces of Chinese honeylocust fruit are peel-removed and roast-dried for 40 to 60 minutes by mudded tile to form radix astragali preparata, afterwards, alumen is put in a fringe with the temperature of minus 20 DEG C for being frozen for 24 hours and then taken out to be ground along with Chinese honeylocust fruit into fine powder, and the fine powder is added with yellow wine and put in a closed jar for three days to obtain product wine. A patient who takes the wine prepared according to the method has own disease symptom prominently recovered within several days.
WO2013091089A9 Three-dimensional cavities of dendritic cell immunoreceptor (dcir), compounds binding thereto and therapeutic applications related to inhibition of human immunodeficiency virus type-1 (hiv-1) The invention is concerned with compounds, pharmaceutical compositions, screening methods, and therapeutic methods for preventing or reducing a human immunodeficiency virus type-1 (HIV-1) infection and/or propagation associated with dendritic cell immunoreceptor (DCIR). Described herein are compounds which bind on at least one three-dimensional cavity of the DCIR, the cavity(ies) being involved in the interaction between HIV-1 and DCIR. Also described are screening methods for identifying active inhibitors and method of using such inhibitors for the prevention or treatment of virus infections, and more particularly for reducing human immunodeficiency virus type-1 (HIV-1) binding, entry and/or replication in human cells.
CN103394047A Special efficacy prescription for treating cervical spondylosi The invention discloses a special efficacy prescription for treating cervical spondylosi, which is composed of the following row materials by weight: 5-15 parts of Cordyceps sinensis, 20-30 parts of ginger, 25-35 parts of Chinese angelica, 12-15 parts of sinapis semina, 2-5 parts of safflower, 5-15 parts of red sage root, 5-10 parts of cassia twig, 5-15 parts of silktree flower, 2-6 parts of pawpaw, 5-15 parts of rhizoma Gastrodiae, 10-25 parts of pseudo-ginseng, 10-20 parts of whole worm, 5-10 parts of rhizoma corydalis, 10-20 parts of juncus roemerianus, and 5-15 parts of borneol. The prescription medicine is prepared by the following steps of: a step 1: crushing Cordyceps sinensis, ginger, Chinese angelica, sinapis semina, safflower, red sage root, cassia twig, silktree flower, pawpaw, rhizoma Gastrodiae, pseudo-ginseng, whole worm, rhizoma corydalis and juncus roemerianu to 100-120 mesh particles, and then uniformly stirring; a step 2: crushing borneol to 80-120 mesh particles, and then adding the borneol into the raw materials of the step 1; and a step 3: filling a mixture obtained in the steps 1 and 2 into a gunny bag, and placing the gunny bag on the cervical vertebra.
US20100008978 Nanoparticles effective for internalization into cells This invention provides antibodies that have improved affinity for the epidermal growth factor receptor (EGFR). In addition, this invention provides microparticles and nanoparticles comprising a plurality of EGFR affinity moieties that are effectively internalized by cells expressing an EGFR.
US7811997 From bamboo using carbon dioxide Supercritical Fluid Extraction; a mixture comprising friedelin,lupenone and homologues; hypotensive agents; anticarcinogenic agents; antitumor agents; free radical scavengers; oxidation resistance; cardiovascular disorders; sin, hair cosmetics; oral administration The invention relates to a composition containing total triterpenoid sapogenins extracted from bamboo, the preparation method and use thereof. These total triterpenoid sapogenins are extracted from many parts of bamboo such as bamboo shavings in Gramineae by CO2 Supercritical Fluid Extraction technique. In the extract, the content of total triterpenoid sapogenins is 10-90%, while the contents of friedelin and lupenone are 5-35% and 1-10%, respectively. The extract in the invention has good physiological and pharmacological activities such as anti-free radical, anti-oxidation, anti-tumor and anti-hypertension. It can be used in medicines or functional foods for the treatment or prevention of cardiovascular and cerebrovascular diseases and tumor. It is also useful in cosmetics field.
WO2012171653A1 Sarizotan for use in the treatment of attention deficit hyperactivity disorder (adhd) The present invention relates to the efficient treatment of an individual afflicted with attention deficit hyperactivity disorder (ADHD), the instant treatment comprising administering to the individual an effective amount of sarizotan or a pharmaceutically acceptable salt thereof.
US20120328627 Chemokine receptor antagonists and use thereof The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
WO2013010102A2 Halogenated phenols for diagnostics, antioxidant protection and drug delivery The present invention provides compositions and methods for the administration and targeted delivery, release and/or formation of a drug compound from a halogenated phenol starting compound of the present invention at site(s) within the body of an individual having high FROS, such as within a diseased and/or inflamed tissue. The present invention further provides compositions and methods for the administration of FROS scavenging compounds to an individual to protect cells and tissues from damage that might be caused by FROS. The present invention further provides compositions and methods for the detection of a detectable product, such as an indigo-like compound or other product of a dehalogenation reaction, formed from a compound of the present invention as a measurement or indication of the amount and/or localization of high FROS levels in the body of an individual.
US20110237670 Improvement of normal cognitive function The present invention shows that administration of L-lysine enhances cognitive performance in healthy individuals directly and these improvements persist if L-lysine is continuously administrated. However, when administration is interrupted the cognitive performance returns to baseline.
US20090023216 Double-Stranded Oligonucleotides Antisense sequences, including duplex RNAi compositions, which possess improved properties over those taught in the prior art are disclosed. The invention provides optimized antisense oligomer compositions and method for making and using the both in in vitro systems and therapeutically. The invention also provides methods of making and using the improved antisense oligomer compositions.
EP1257551B1 Heterocyclic compounds and their use as parp inhibitors The invention relates to compounds of formula (I), wherein; either A1 or A2 represents CONH¿2?, and the other radical A?2 or A1¿ represents hydrogen, chlorine, fluorine, bromine, iodine C¿1?-C6 alkyl, OH, nitro, CF3, CN, NR?11R12¿, NH-CO-R13, O-C1-C4 alkyl; X1 can represent N and C-R2; X2, independent of X1, can represent N and C-R2; R2 can represent hydrogen, C¿1?-C6 alkyl, C1-C4 alkyl-phenyl, phenyl; B can represent an unsaturated, saturated or partially unsaturated monocyclic, bicyclic or tricyclic ring having a maximum of 15 carbon atoms, an unsaturated, saturated or partially unsaturated monocyclic, bicyclic or tricyclic ring having a maximum of 14 carbon atoms and 0 to 5 nitrogen atoms, 0 to 2 oxygen atoms or 0 to 2 sulfur atoms, which can each still be substituted with an R?4¿ and a maximum of 3 of the same or different radicals R5, and; R?1, R4, R5, R11-R13¿ have the meanings as cited in Claim No. 1. The invention also relates to the tautomeric forms, and possible enantiomeric and diastereomeric forms of said compounds, to the prodrugs thereof and to their use as PARP inhibitors.
US7566552 Protection against environmental toxicity through manipulation of the processing of messenger RNA precursors This invention describes the identification of pre-messenger RNA processing as a novel target of environmental stress caused for example by lithium and sodium toxicity. Overexpression of different types of proteins (or protein fragments) from different organisms but all involved in pre-mRNA processing, protects yeast from salt stress, which indicates that any stimulation of this process, independently of its mechanism, may counteract the toxic effects of mineral salts. A similar phenotype of tolerance to NaCl and to LiCl has been observed by overexpression of these types of proteins in transgenic Arabidopsis plants, demonstrating the generality of this protective effect in eukaryotic cells and organisms.
WO2012101173A1 N-methyl-2-pyrrolidone for prevention and treatment of bone loss The invention provides N-Methyl-2-pyrrolidone for the prevention and treatment of bone loss, particularly for osteoporosis.
US7943157 copolymer based on acryloxydimethyltaurine; water soluble, water swelling The invention provides cosmetic, pharmaceutical and dermatological compositions comprising at least one copolymer obtainable by free-radical copolymerization of A) acryloyldimethyltaurine and/or acryloyldimethyltaurates, B) optionally, one or more further olefinically unsaturated, noncationic comonomers, C) optionally, one or more olefinically unsaturated, cationic comonomers, D) optionally, one or more silicon-containing components, E) optionally, one or more fluorine-containing components, F) optionally, one or more macromonomers, G) the copolymerization taking place if desired in the presence of at least one polymeric additive.
CN103271887A Furazolidone tablet preparation method The present invention relates to a furazolidone tablet preparation method, which is performed according to the following steps: taking furazolidone, a binder and a solubilizer, screening, respectively screening a lubricant and a flow aid with a 80-120 mesh sieve, adding water or an alcohol to the partial binder having the content of more than or equal to 28% of the total amount of the binder and the partial solubilizer having the content of more than or equal to 14% of the total amount of the solubilizer to prepare a binder solution with a mass concentration of 1-30%, uniformly mixing the remaining binder and the remaining solubilizer, uniformly mixing with the furazolidone according to an equivalent gradual increase method, adding the binder solution to prepare a soft material, carrying out 12-30 mesh pelletization, drying at a temperature of less than 70 DEG C, carrying out 12-30 mesh granulating, adding a lubricant and a flow aid, uniformly mixing, and tabletting to obtain the finished product. According to the present invention, the reasonable process operation sequence is adopted, the part of the solubilizer is adopted to increase furazolidone hydrophilicity, and the part of the solubilizer is adopted to promote furazolidone self-emulsifying and increase solubility in water so as to improve a dissolution rate and increase bioavailability.
US7943643 Aryl substituted pyridines and the use thereof This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1-R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
CA2504078C Treatment of chemotherapeutic agent and antiviral agent toxicity with acylated pyrimidine nucleosides The subject invention discloses compounds, compositions and methods for treatment and prevention of toxicity due to chemotherapeutic agents and antiviral agents.Disclosed are acylated derivatives of non-methylated pyrimidine nucleosides. These compounds are capable of attenuating damage to the hematopoietic system in animals receiving antiviral or antineoplastic chemotherapy.
US20060247439 Mchir antagonists The present invention provides compounds of formula (I), wherein R1 represents a C1-4 alkoxy group optionally substituted by one or more fluoro or a C1-4alkyl group optionally substituted by one or more fluoro; n represents 0 or 1; R2 represents a C1-4alkyl group optionally substituted by one or more fluoro or a C1-4alkoxy group optionally substituted by one or more fluoro; m represents 0 or 1; R3 represents H or a C1-4alkyl group; L1 represents an alkylene chain (CH2)r in which r represents 2 or 3 or L1 represents a cyclohexyl group wherein the two nitrogens bearing R3 and R4, respectively, are linked to the cyclohexyl group either via the 1,3 or the 1,4 positions of the cyclohexyl group or L1 represents a cyclopentyl group wherein the two nitrogens bearing R3 and R4, respectively, are linked to the cyclopentyl group via the 1,3 position of the cyclopentyl group and additionally when R5 represents 9,10-methanoanthracen-9(10H)-yl the group -L1-N(R4)— together represents a piperidyl ring which is linked to L2 through the piperidinyl nitrogen and to N—R3 via the 4 position of the piperidyl ring with the proviso that when R5 represents 9,10-methanoanthracen-9(10H)-yl then r is only 2; R4 represents H or a C1-4alkyl group optionally substituted by one or more of the following: an aryl group or a heteroaryl group; L2 represents a bond or an alkylene chain (CH2), in which s represents 1, 2 or 3 wherein the alkylene chain is optionally substituted by one or more of the following: a C1-4alkyl group, phenyl or heteroaryl; R5 represents aryl, a heterocyclic group or a CH3-8cycloalkyl group which is optionally fused to a phenyl or to a heteroaryl group; as well as optical isomers and racemates thereof as well as pharmaceutically acceptable salts, thereof; with provisos, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders and to pharmaceutical compositions containing them.
US7109011 Nucleotide sequences coding polypeptide for use in the treatment of infections, pneumonia, toxic shock, brain and rheumatic diseases The present invention relates to a nucleic acid segment having a coding region segment encoding enzymatically active Streptococcus equisimilis hyaluronate synthase (seHAS), and to the use of this nucleic acid segment in the preparation of recombinant cells which produce hyaluronate synthase and its hyaluronic acid product. Hyaluronate is also known as hyaluronic acid or hyaluronan.
US20080085930 Characterized by a powder X-ray diffraction pattern having one powder X-ray diffraction peak at about 10.0 degrees 2-theta; useful for treating and/or preventing central nervous system disorders such as epilepsy, stroke, muscle spasms, neuropathic pain, and migraine The present invention relates to a novel crystal of (S)-(+)-2-(2-chlorophenyl)-2-hydroxy-ethyl carbamate, pharmaceutical compositions comprising this crystal and, and methods of making and using this crystal.
US20080214597 Tricyclic Lactam Derivatives as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents C or N; Y represents C or N; L represents a methyl or a direct bond; Z1 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b); Z2 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b); R1 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR3R4 or C1-4alkyl optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR5R6 or R1 represents C1-4alkyloxy- optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR7R8; R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-; R3 and R4 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R5 and R6 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R7 and R8 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; A represents phenyl or a monocyclic heterocycle selected from the group consisting of thiophenyl, furanyl, oxazolyl, thiazolyl, imidazolyl, isoxazolyl, isothiazolyl, pyrridinyl, pyridazinyl, pyrimidinyl and piperazinyl.
WO2009151152A1 Oxycarbamoyl compounds and the use thereof The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockadeof calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
US20110160152 Extracts of aquilaria hulls and use thereof in the treatment of cancer The invention discloses an ethyl acetate layer of methanol extract of Aquilaria hulls for killing cancer cells and treating/preventing cancers and its uses. The extracts of Aquilaria hulls has an significant amount of cucurbitacins and these cucurbitacins are effective in killing cancer cells and treating/preventing cancers.
CN103417514A Microencapsulated butylphthalide medicine composition, preparation method and applications The invention relates to a microencapsulated butylphthalide medicine composition, a preparation method and applications. Butylphthalide is microencapsulated to raise the solubility of butylphthalide, prevent volatilization, develop required solid preparations and liquid preparations clinically and give play to therapeutical effects of butylphthalide better. The composition contains butylphthalide effective component with a mass percent of 1-55%. Butylphthalide is coated with natural or synthesized high polymer materials as capsule wall materials or carrier materials to form microencapsules. The composition can be prepared into various preparations of powder, capsules, chewable tablets, buried tablets, buccal tablets, other oral compressed tablets, injection, liquid suspension, lotion, powder-injection, coating preparations, thin film preparations and the like.
CN103664690A Acylhydrazone derivatives of protocatechuic acid, and preparation method and antibacterial activity thereof The invention discloses acylhydrazone derivatives of protocatechuic acid, of which the general formula is disclosed in the specification, wherein R is disclosed in the specification. The acylhydrazone derivatives of protocatechuic acid have different inhibiting actions on B. subtilis, S. aureus, E. coli and P. aeruginosa, and thus, can be used in preparing antibacterial drugs. The invention also discloses a preparation method of the acylhydrazone derivatives of protocatechuic acid.
CN103405422A Application of Chukrasone B in medicine for treating cholangiocarcinoma The invention discloses application of Chukrasone B in preparation of a medicine for treating human cholangiocarcinoma, and belongs to the technical field of new application of medicines. The in-vitro MTT (3-4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) antitumor activity evaluation shows that Chukrasone B has remarkable inhibition effect on the growth of human cholangiocarcinoma cell line REB, so that Chukrasone B has a good development and application prospect and can be applied to the preparation of the medicine for treating the cholangiocarcinoma. The application of Chukrasone B in the preparation of the medicine for treating human cholangiocarcinoma is disclosed for the first time; the framework type of Chukrasone B is brand new; Chukrasone B brings unexpected inhibition activity for human cholangiocarcinoma cells.
US20120252887 Composition and method for treating diabetes and metabolic disorders A composition and method for treating diabetes and metabolic disorders, and for achieving weight loss in a subject comprising a combination of naturally occurring compounds is provided.
US20110065776 Method for Treating Hepatitis C Infection The present invention relates to a method for treating hepatitis C virus (HCV) infection, comprising administrating a subject in need thereof with a therapeutically effective amount of an inhibitor against a serine/threonine kinase (AKT) and an activator thereof. A method for screening a candidate agent for treating hepatitis C infection determined by the presence of an inhibition of AKT function is also provided.
DE102007032664A1 Cosmetic or dermatological preparations for skin care, protection and cleaning, containing apiogalacturonan compounds or extracts thereof from seaweed, together with molecular oxygen Preparations containing one or more apiogalacturonans (I) or extract(s) of (I) from Zostera marina and also containing molecular oxygen.
EP1779850A1 Tgf- gene expression inhibitor A TGF-β gene expression inhibitor containing a pyrrole-immidazole polyamide comprising an N-methylpyrrole unit (hereinafter also referred to as Py), an N-methylimidazole unit (hereinafter also referred to as Im) and a γ-aminobutyric acid unit which can be folded into an U-shaped conformation at the above-described γ-aminobutyric acid unit site in a minor groove of a double-stranded region (hereinafter referred to as the target region) containing a part or the whole of the following base sequence (SEQ ID NO: 2) corresponding to -450 to -310 of human transforming growth factor β1 (hereinafter also referred to as h TGF-β1) promoter and a strand complementary thereto and in which a Py/Im pair, an Im/Py pair and a PY/Py pair correspond respectively to a C-G base pair, a G-C base pair and an A-T base pair and a T-A base pair.
US7064112 selectively inhibiting abnormal cell proliferation by administering an A3-selective adenosine A3 receptor agonist in an amount of less than 100 mu g/Kg body weight. Adenosine receptor agonists, particularly an agonist which binds to the A3 adenosine receptor, are used for induction of production or secretion of G-CSF within the body, prevention or treatment of toxic side effects of a drug or prevention or treatment of leukopenia, particularly drug-induced leukopenias; and inhibition of abnormal cell growth and proliferation.
US20090074833 Bridged polycyclic compound based compositions for controlling bone resorption A pharmaceutically active agent, a pharmaceutically active agent carrier and method of use thereof are described. In some embodiments, a system may include a composition. The composition may include one or more bridged polycyclic compounds. At least one of the bridged polycyclic compounds may include at least two cyclic groups, and at least two pharmaceutically active agents may be associated with the bridged polycyclic compound. In some embodiments, a composition may be administered to a subject to control bone resorption, inflammation, and/or pain.
US20060116339 Antisense modulation of purinoreceptor p2x3 The invention relates to antisense oligonucleotides, compositions and methods useful for modulating the expression of P2X3. The compositions comprise antisense oligonucleotides, particularly antisense oligonucleotides targeted to nucleic acids encoding P2X3.
WO2013026383A1 Tetrandrine derivatives with substituted 5-carbon, preparation method and use thereof The present invention belongs to the field of natural medicine and medicinal chemistry, in particular relating to novel tetrandrine derivatives with substituted 5-carbon of general formula (I) or pharmaceutically acceptable adducts, complexes and salts thereof, to preparation methods therefor, to pharmaceutical compositions containing the compound, and to use thereof in preparing antitumour drugs.
US20050042733 Propagating swine mast cells in nutrient broth and recovering mucopolysaccharides/heparin The invention concerns the production of heparin from mast cell cultures, in particular pig mast cells.
WO2006132177A1 Human cell differentiation inducer and product containing the same A human cell differentiation inducer containing a glyceride form of Ϝ-linolenic acid. This differentiation inducer has fewer side effects and also has an excellent function of inducing/promoting human cell differentiation thereby to promote an action of promoting epidermal melanin excretion and cell turnover, therefore it can be used in a dermatological agent, a cosmetic product, a food or the like.
US8309570 E.g., dextromethorphan hydrobromide, amantadine, memantine, remacemide or riluzole; treating pain resulting from injury, trauma, lesion or other disorders in the spinal cord or brain Central neuropathic pain is treated with an analgesic composition that consists essentially of an N-methyl-D-aspartate (NMDA) receptor antagonist. In one embodiment, the invention includes chronic administration of the (NMDA) receptor antagonist. In another embodiment, the invention is use of an NMDA receptor antagonist or component thereof for the manufacture of a medicament than includes an analgesic component that consists essentially of an NMDA receptor antagonist for the chronic treatment of central neuropathic pain.
WO2012011572A1 Therapeutic agent for diastolic heart failure It has been discovered that carnitine, a derivative thereof or a pharmaceutically acceptable salt thereof is useful as an active ingredient of a prophylactic or therapeutic agent for diastolic heart failure. The present invention is capable of providing a pharmaceutical agent that is effective for prophylaxis or treatment of diastolic heart failure, on which an effective therapeutic method has not been established yet.
CN1593659A Coupled compound of 5-methyl-morpholine-3-amino-2-oxazolidinone and preparation method thereof The invention discloses a 5-methylmorpholine-3-amido-2-oxazolidinone (AMOZ) coupling substance with a general formula (I), which is composed by optimizing cow serum protein from 5-methylmorpholine-3-amino-2-oxazolidinone and carrying agent substance for producing immunogen performance, wherein n is the number of molecules of AMOZ combining with a cow serum protein, BSA is cow serum protein, its molecular weight range is between 6.6KDa-6.9KDa. The invention also discloses the process for preparing the coupling substance.
WO2008120070A3 2(hydroxyethyl)trimethylammonium thioctate (choline thioctate) displaying hepatoprotective, hypoammoniemic and detoxic action, a method for its production and a pharmaceutical composition based thereon The invention relates to medicine and chemical and pharmaceutical industry, and more particularly to a new physiologically active substance 2(hydroxyethyl)trimethylammonium thioctate (choline thioctate) displaying hepatoprotective, hypoammoniemic and detoxic activity, to a method for producing said substance, and to pharmaceutical compositions based thereon. The technical result of implementing the invention is a new physiologically active chemical substance 2(hydroxyethyl)trimethylammonium thioctate (choline thioctate) displaying hepatoprotective, hypoammoniemic and detoxic activity, a method for producing the same which method ensures a higher level and a wider spectrum of specific activity while simplifying, and shortening the duration of the manufacturing process, and pharmaceutical compositions based on the new physiologically active substance 2(hydroxyethyl)trimethylammonium thioctate (choline thioctate) in various dosage forms the use whereof results in a diversified range of hepatoprotective drugs.
US20100029758 Derivatives of isoflavones The present invention discloses novel isoflavone conjugates and their use for affinity targeting of drugs, imaging and detection agents to cells having estrogen receptors, particularly estrogen receptors subtype β.
US20070281958 Preparation of oxycodone A process for preparing oxycodone or an oxycodone salt, wherein the oxycodone or oxycodone salt has low levels of impurities (especially 14-hydroxycodeinone) is disclosed. The process comprises the steps of: a) preparing a mixture comprising oxycodone and a solvent and adjusting the pH of the mixture to less than 6; and subsequently b) exposing the mixture to hydrogenation reagents for a period of at least 1 hour. This process provides oxycodone with very low levels of α,β-unsaturated ketone impurities. Oxycodone or an oxycodone salt produced according to the process of the invention has low levels of α,β-unsaturated ketones and is advantageously incorporated into pharmaceutical products.
CN1981749A Use of beta-elemene for inhibiting cerebrovascular endothelial cell An application of beta-elemene in suppressing the cerebrovascular endothelial cells with high selectivity and in turn the cerebral tumor and cerebral metastatic tumor, and treating the cerebral tumor and cerebral metastatic tumor is disclosed.
US7256199 2-(Substituted amino)-6-(4-pyridyl)pyrimidin-4-ones, e.g., 2-(N-phenylamino)-6-(4-pyridyl)pyrimidin-4-one and 2-(N-(3-bromophenyl)amino)-6-(4-pyridyl)pyrimidin-4-one; treatment of diseases caused by tau protein kinase 1 hyperactivity such as Alzheimer disease. A pyrimidone derivative represented by the formula (I) or a salts thereof: wherein R1 represents an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group and the like; R2 represents a hydrogen atom, hydroxyl group, an alkyl group, an alkenyl group and the like, R3 represents a pyridyl group, and a medicament comprising said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as Alzheimer disease.
CN103102302A Quinolinone compound, preparation method and pharmaceutical composition of quinolinone compound and application of pharmaceutical composition The invention provides a novel quinolinone compound called after morpholine ketone of which the chemical structure is shown in formula I, the name is 2-undecyl-3-methyl-4(1H)-quinolinone and the chemical formula is C21H31NO. The invention also provides an application of a pharmaceutical composition of the compound in preparation of a medicament for preventing and/or treating a gastritis disease caused by helicobacter pylori. The N at a first site of the quinolinone is not hydroxylated, and the N at a second site of the quinolinone is substituted by undecyl. The quinolinone is completely synthesized. The compound I has a highly-selective inhibiting effect on the helicobacter pylori and can also be used as an efficient proton pump inhibitor, so that the probability of developing a new medicament for treating the gastritis disease caused by the helicobacter pylori is provided.
CN101347229A Health care food with intestine-moistening and bowel-relaxing functions and production method The invention provides a healthcare food with the function of moistening the intestine to relieve constipation and a production method thereof, which particularly relates to the field of healthcare foods, in particular to a healthcare food which takes glucomannan as a main material and can improve intestinal function, and the production method thereof. The invention provides a healthcare food which has the function of moistening the intestine to relieve constipation, takes the glucomannan as the main material, and can improve the intestinal function and the production method thereof. The healthcare food is characterized by containing the glucomannan, fructooligosaccharide and isomaltooligosaccharide.
WO2011115585A1 Pharmaceutical combination of acetylsalicylic acid and antifungal compound for destroying or growth inhibition and reproduction of fungi The presented invention relates to a pharmaceutical combination of an antifungal substance and salicylic or acetylsalicylic acid, salt or derivative thereof to enhance fungicidic or fungistatic efficiency of the antifungal substance for treating or preventing fungal infection. The invention refers to a medicament or a plant protection product, which contains the pharmaceutical combination and a method for preventing fungal infections in vitro for the disinfection of surfaces and implants.
US7030136 Administering phanquinone to the subject, optionally together with one or more pharmaceutically acceptable carriers for improving the learning or memory of a normal subject The use of phanquinone (4,7-phenanthroline-5,6-dione) for the treatment or prevention of memory impairment is suggested. Also a method for improving the learning or memory of a normal subject is suggested, said method comprising the administering of phanquinone, optionally together with one or more pharmaceutically acceptable carrier(s).
US20110268775 Nanoparticle pharmaceutical formulations The present invention is directed to methods of preparing nanoparticles of aqueous-insoluble compounds, particularly aqueous-insoluble bioactive (drug) compounds, and to compositions and medicaments obtained by these methods. These methods, compositions, and other inventive aspects of the present invention are based particularly on the use of bile acid compound(s) to prepare nanoparticles of aqueous-insoluble compounds.
WO2009091788A1 3h-[1,2,3]triazolo[4,5-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses The invention relates to 3H-[1,2,3]triazolo[4,5-d]pyrimidine compounds of the Formula 1 or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
US7371895 antiinflammatory agents; autoimmune and cardiovascular disorders; atherosclerosis, rheumatoid arthritis, hyperlipemia; better water solubility increases the bioavailability and pharmacokinetics Organic amine salts of compounds of the formula: and their pharmaceutically acceptable salts, and uses in medical therapy are provided.
WO2012142256A3 Modulators of mitochondrial protein import The present invention provides compounds that modulate protein translocation in mitochondria, compositions thereof, and methods of identifying, making and using these.
US20100113485 Piperidinylamino-thieno[2,3-D] Pyrimidine Compounds The invention relates to 5-HT receptor modulators, particularly 5-HT2B antagonists. Novel piperidinylamino-thieno[2,3-d]pyrimidine compounds represented by Formula I, II and III, and uses thereof for treating conditions including pulmonary arterial hypertension, congestive heart failure, and hypertension.
US20100297227 Pharmaceutical composition comprising at least one active agent and a binder, which swells in an acidic media The invention relates to a pharmaceutical composition, which comprises at least one active agent and which further comprises a binder and/or a retarding agent, wherein the binder swells in an acidic medium, and the retarding agent retards the release of the active agent in an acidic or alkaline medium.
EP0949919B1 A process for stabilizing levogyre ascorbic acid (laa) and stable laa compositions The present invention refers to a process for stabilyzing LAA in an aqueous medium, which comprises the step of contacting the LAA with at least one compound capable of forming hydrogen bridges with the LAA. In another aspect, the invention relates to a stable aqueous LAA composition which comprises, in addition to said ascorbic acid, at least one compound which is linked to the LAA by hydrogen bridges, and to a process for preparing it. The present invention further relates to an emulsion including, in its aqueous phase, at least one compound linked to levogyre ascorbic acid (LAA) by hydrogen bridges. Further according to the present invention, a vitamin product is provided, in which a stable LAA composition as described above is contained in organic envelopes which enable a gradual and prolonged release of said LAA into the organism. Said vitamin product may further comprise a compound capable of stimulating the metabolism of the fibroblasts. The present invention further relates to a method for cosmetic, therapeutic or nutritional treatment, which comprises the administration of a composition as described above.
CN101843616A Composition of fexofenadine hydrochloride and microcrystalline cellulose and preparation method thereof The invention relates to a composition of fexofenadine hydrochloride and microcrystalline cellulose. On the basis of totally manufacturing 1000 chips, the composition comprises the following components: 60 grams of the fexofenadine hydrochloride, 66 grams of the microcrystalline cellulose, 34 grams of starch, 10 grams of sodium carboxymethyl cellulose, proper quantity of 5-pecent povidone ethanol solution, and 0.8 gram of magnesium stearate; and on the basis of totally coating 1000 film coats, the composition comprises the following components: 0.67 gram of hydroxypropyl methylcellulose, 0.33 milliliter of propylene glycol, 800.33 milliliters of polysorbate, 0.67 gram of titanium dioxide, 26.7 milliliters of 95-percent ethanol and 6.67 milliliters of purified water. The method for preparing the composition comprises staged production steps. As both the microcrystalline cellulose and the starch have high fluidity and compressibility and can accelerate disintegration of tablets, the microcrystalline cellulose and the starch are selected and used on the basis of determining the used amount of the fexofenadine hydrochloride; and the sodium carboxymethyl cellulose is selected as a disintegrating agent, has higher disintegration and higher compressibility, and is an excellent disintegrating agent for the tablets.
CN102670598A Penicillin borneol composition The invention discloses a penicillin borneol composition, which belongs to the technical field of preparation of medicaments. The penicillin borneol composition consists of penicillin and borneol in the mass ratio of 1:0.1-1:10, wherein the optimal mass ratio is 1:1. The composition can be prepared into various dosage forms such as tablets, capsules, particles, a sustained release agent, an injection and the like together with pharmaceutically-general auxiliary materials with the conventional medicament preparation method. The composition has a good inhibiting action on a plurality of medicament-resistant bacteria and a wide application prospect; and the order of magnitude of the MIC (Minimal Inhibitory Concentration) value is lowered, so that phenomenon of medicament resistance existing in the conventional antibiotics is greatly improved.
CN1911208A Injection of Jiabei mesylate and its prpen. method An injection of gabexate mesilate is prepared through dissolving gabexate mesilate in 1,2-propanediol, adding sodium chloride, sodium sulfite and the water for injection, stirring, adding PEG400, stirring, adding the water for injection, regulating pH=4-5, adding the activated carbon for injection, stirring, laying aside, filtering for removing carbon, examining, fine filtering, aerating N2, filling it in ampules, steam sterilizing, examining and packing.
US20120283225 Combination Therapy for Skin Disorders The present invention provides a novel therapeutic combination comprising one or more anti-androgen agents and one or more antibiotic/anti-inflammatory agents or pharmaceutically acceptable salts or hydrates thereof, useful for the treatment of a dermatological disorder.
CN102389397A Preparation method of ibuprofen enteric particles The invention belongs to the technical field of medicine and provides a preparation method of ibuprofen enteric particles. Ibuprofen is a nonsteroidal anti-inflammatory medicament and can be dissolved in alkaline solution, polyacrylic resin III also can be dissolved in the alkaline solution, and the ibuprofen enteric particles are prepared by utilizing the property and adopting a method of changing a pH value. The preparation method has the advantages of simple technological operation, good repeatability and high yield, and is suitable for industrialized production.
CN103641829A Triazole derivatives as kinase inhibitors The invention relates to compounds of formula (I); wherein X and R1 to R5 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of Itk or PI3K, for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
US20100062971 such as 2-{3-[2-(4-Methoxy-phenyl)-ethyl]-6-methyl-1H-indazol-4-yloxy} beta -D-glucopyranoside, used for for treating diabetes, Syndrome X, obesity, nephropathy, neuropathy, retinopathy, atherosclerosis, polycystic ovarian syndrome, hypertension, ischemia, stroke and cardiovascula disorders Substituted indazole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.
WO2013133556A1 Novel triazolo pyridazine derivative and use therefor The present invention relates to a novel triazolo pyridazine derivative or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition for inhibiting c-Met tyrosine kinase activity and a pharmaceutical composition for preventing or treating an abnormal proliferation disorder (hyperproliferative disorder) comprising same as an active ingredient, and to a method for preventing or treating an abnormal proliferation disorder (hyperproliferative disorder) comprising a step of administering a pharmaceutically effective amount of the pharmaceutical composition to a subject in need thereof. The present invention can advantageously be used as a therapeutic agent for various abnormal proliferation disorders such as cancer, psoriasis, rheumatoid arthritis and diabetic retinopathy which are associated with excessive cell proliferation and growth due to irregular kinase activity by effectively suppressing the activity of c-Met tyrosine kinase.
CN101676287A 6-(substituted phenoxy)-tetrazolo[5,1-a] phthalazine derivatives as antuepileptics and their pharmaceutically acceptable salts A compound represented by a general formula I, and salts formed by the addition reaction of the same and the pharmaceutically acceptable acids, wherein, R is selected from various halogenated alkanes.The compound represented by the general formula I and salts formed by the addition reaction of the same and the pharmaceutically acceptable acids, provided by the invention, can be used for treatingepilepsy.
CN1721403A Water soluble bilirubin and its synthesis process and use The present invention relates to new compound, and is especially one kind of water soluble cholerythrin and its synthesis process and use. Cholerythrin is made to combine with matter with hydrophilic group to form one new matter comprising cholerythrin and two hydrophilic groups, and the new matter may be used in preparing medicine for preventing and treating cardiac, cerebral and nephric vascular diseases and Parkinson's disease.
CN103655596A Application of CpG-ODN 7909 sequence to preparation of drug for relieving tumor cell radiation tolerance The invention provides an application of a CpG-ODN 7909 sequence to the preparation of a drug, i.e., a radiosensitizer for relieving tumor cell radiation tolerance. The CpG-ODN 7909 sequence is 5'-TCGTCGTTTTGTCGTTTTGTCGTT-3' and takes non-methylated cytosine guanine dinucleotide as a core. The CpG-ODN 7909 sequence is proved to be capable of remarkably reducing the growth speed of a radiation-resistant cell system, delaying the cell period, enhancing the radiation sensibility and lowering the radiation tolerance with the assistance of radiation, so that the CpG-ODN 7909 sequence can be used as the radiosensitizer to treat tumor with the assistance of radiation, can be used for achieving a favorable treating effect and has a wide application prospect.
WO2012042042A1 Selective lsd1 and dual lsd1/mao-b inhibitors for modulating diseases associated with alterations in protein conformation The invention relates to methods and compositions for the treatment or prevention of protein conformation disorders. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing a protein conformation disorder, such as, e.g., Huntington Disease.
WO2014057266A1 Acylpiperazines as inhibitors of transglutaminase and their use in medicine The present invention relates to novel compounds of Formula I capable of inhibiting tissue transglutaminase, and uses of the same in medicine. In particular, the invention provides compounds for use in the treatment of prevention of disease and conditions such as fibrosis (e.g. cystic fibrosis), scarring, neurodegenerative diseases (e.g. Alzheimer's disease, Huntington's disease and Parkinson's disease), autoimmune diseases (e.g. multiple sclerosis and coeliac disease), thrombosis, proliferative disorders (e.g. cancers), AIDS, psoriasis and inflammation (e.g. chronic inflammatory diseases).
WO2010145197A8 Novel 6-arylamino pyridone sulfonamides and 6-arylamino pyrazinone sulfonamdies as mek inhibitors The invention provides novel substituted 6-arylamino pyridone sulfonamides and 6 arylamino pyrazinone sulfonamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.
US20070219233 Substituted Indoles and Their Use as Integrin Antagonists The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
US20110003790 Pyrido [4, 3-d] pyrimidinone derivatives as kinase inhibitors The invention provides a class of compounds of Formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC, IGR-IR, AIk, c-FMS, or combinations thereof.
WO2012113920A1 Arylsulfone derivatives with activity against human betaherpesviruses The present invention relates to compounds and compositions having antiviral activity, in particular antiherpes activity, more in particular antibetaherpes activity. The compound of the invention is of formula (I), or a tautomer thereof, or a pharmaceutically acceptable salt or solvate of said compound or tautomer thereof, wherein R1, R2, R3, R4, R5 and R6 have defined meanings.
EP1495019B1 Glucopyranoside, process for isolation thereof, pharmaceutical composition containing same and use thereof A novel glucopyranoside, 6-hydroxy-2-p-hydroxybenzylbenzofuran-7-C-β-D-glucopyranoside of the formula (1) isolated from Pterocarpus marsupium and to a process for the isolation thereof is disclosed. The invention also relates to a pharmaceutical composition containing 6-hydroxy-2-p-hydroxybenzylbenzofuran-7-C-β-D-glucopyranoside and to method for the treatment of diabetes using said compound.
US8637535 Polymorphic and other crystalline forms of cis-FTC Solid phases of (−)-cis-FTC, which are designated herein as amorphous (−)-FTC and Forms II and III (−)-cis-FTC) are provided that can be distinguished from Form I (−)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.
US20110082090 Compounds suited as nanocarriers for active agents and their use The invention relates to a compound suited as entity carrier, having the general formula (I) wherein X is an amine-containing residue further defined herein. The invention further relates to the use of such compounds, a nanocarrier system, a kit comprising such compounds and methods for gene silencing and anti-cancer treatment.
US20130034495 Isotopologues of 4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro-phenylamino)-9h-purin-2-ylamino]-cyclohexan-1-ol Provided herein are isotopologues of Compound 1, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.
US7482320 Modulation of smooth muscle cell proliferation There is provided a novel use for vascular endothelial growth factor, herein designated VEGF-X, and a CUB domain present in the sequence of VEGF-X, which enhance smooth muscle cell proliferation and can be used to treat diseases associated with reduced smooth muscle cell proliferation. VEGF-X, and a CUB domain can also be used in tissue engineering applications to increase the number of smooth muscle cells within specific tissue to restore that tissue function or architecture. Screening methods for identifying inhibitors of VEGF-X biological activity are also disclosed and these inhibitors include neutralizing VEGF-X antibodies, antisense VEGF-X sequences or non-protein antagonists competing with VEGF-X biological activity. Also provided are therapeutic methods for treating disorders associated with smooth muscle cells hyperproliferation and methods of diagnosis a pathological condition or susceptibility to a pathological condition associated with smooth muscle cell hyperproliferation.
CN102139004B Plaster for treating gout disease and application thereof The invention discloses a plaster for treating a gout disease. The plaster comprises an ointment A and a paeonol ointment. The invention has good effect, preparation reasonability and convenience in preparation.
WO2011107019A1 Antibacterial compounds, preparation methods and uses thereof Antibacterial compounds, preparation methods and uses thereof are disclosed. Said compounds are N-[[3-[3-Fluoro-4-[4-[2-hydroxyl-3-(2-methyl-5-nitro-1H-imidazol- 1-yl) propyl]piperazin-1-yl]phenyl]-2-oxazolidinon-5-yl]methyl] acetamide, its enantiomers, diastereoisomers, mixture of enantiomers, N-oxides and pharmaceutically acceptable salts, hydrates, solvates or prodrugs.
US20080161251 Combination of a cytotoxic agent such as gemcitabine and a compound that inhibits cyclin dependent kinase (CDK) and/or glycogen synthase kinase (GSK, e.g. GSK-3) such as 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide The invention provides a combination of a cytotoxic compound or signalling inhibitor and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NRg(C═O) or 0(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).
CN102309440A Method for producing ganciclovir glucose injection The invention belongs to the field of pharmaceutical preparations and in particular relates to a method for adjusting a pH value in the process of producing ganciclovir glucose injection. The method for producing the ganciclovir glucose injection is characterized by comprising the following steps: adding a pH value buffering agent in the process of preparing the ganciclovir glucose injection; adding the pH value buffering agent or corresponding weak acid according to the initially adjusted pH value of the ganciclovir glucose injection; and adjusting the pH value again to be within the required range. According to the ganciclovir glucose injection produced by using the method disclosed by the invention, the pH value of a finished product after being sterilized is slightly reduced; a few related substances are generated; and the quality is better.
WO2011015953A3 Greater utility with thyroid hormone Formulations and delivery systems that include a thyroid hormone active agent consisting essentially of T4 should reduce fluctuations in delivery of thyroid hormone.
WO2010065787A3 Treatment of tumor suppressor gene related diseases by inhibition of natural antisense transcript to the gene The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Tumor Suppressor genes, in particular, by targeting natural antisense polynucleotides of Tumor Suppressor genes. The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of Tumor Suppressor genes.
CN101147725A Ketoconazole suppository composition for vaginal administration The present invention relates to a suppository composition. Said suppository composition includes its medicine active component ketoconazole and preparation excipient containing specific hydrophilic suppository matrix.
WO2012143320A1 (7h-pyrrolo[2,3-d]pyrimidin-2-yl)amine compounds as jak3 inhibitors The present invention relates to compounds of formula (I) wherein X1 to X5, Y, and Z1 to Z3 have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
WO2013170069A1 Medicament, method, and drug delivery device for treatment of ovarian cancer Drug delivery devices, medicaments, and methods are provided for the intraperitoneal treatment of ovarian cancer. An implantable device for drug delivery includes an elongated, flexible device having a housing defining a reservoir that contains a drug in solid or semi-solid form, and configured to be wholly deployed within the peritoneal cavity of a patient and continuously release a therapeutically effective amount of the drug over a period of at least 24 hours. A medicament includes cisplatin for administration into the peritoneal cavity of a patient continuously over a treatment period of at least 24 hours. A method of drug delivery includes implanting within the peritoneal cavity of a patient an elongated, flexible device having a reservoir containing a drug, solubilizing the drug at least in part with peritoneal fluid, and releasing an effective amount of the solubilized drug from the reservoir continuously for a period of at least 24 hours.
CN101099725A Method for preparing composite substrate multifunctional arterial embolic agent The present invention relates to a preparation method of multifunctional arterial embolism preparation combined with matrix. Said preparation method includes the following steps: making doxorubicin hydrochloride be dispersed in an oily contrast medium, under the action of surfactant making them be formed into microemulsion or submicroemulsion and using it as primary emulsion phase E1; making the primary emulsion phase be uniformly dropped into W phase of sodium alginate solution containing surfactant and calcium carbonate or calcium phosphate micropowder so as to form secondary emulsion E2; then making the secondary emulsion be uniformly dropped into a liquid paraffin so as to obtain final emulsion E3, under the condition of continuously stirring adding organic acid, implementing cross-linking and balling reaction, making precipitation and removing upper layer liquor so as to obtain the invented microball embolism preparation containing chemicotherapeutic medicine and radiodeveloper.
US7495003 e.g. 1-(naphthyl-1-ylmethyl)-3-(methoxycarbonylmethyl)-7-(but-2-ynyl)-8-(3-amino-piperidin-1-yl)-xanthine; dipeptidyl-peptidase-IV (DPP-IV) inhibitor; antidiabetic, diuretic, antihypertensive agent; insulin resistance, obesity; irritable bowel syndrome (IBS), Crohn's disease, ulcerative colitis The application relates to new substituted xanthines of general formula wherein R1 and R2 are defined as in claims 1 to 11, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
WO2014075391A1 Platinum compound of malonic acid derivative having leaving group containing amino or alkylamino Disclosed are a platinum compound of malonic acid derivative having a leaving group containing an amino or alkylamino, and pharmaceutically acceptable salt thereof, preparation method thereof and pharmaceutical composition containing the compound. Also disclosed are uses of the compound for treating cell proliferative diseases especially cancers. The platinum compound of the present invention has high solubility in water, low toxicity and strong anti-tumor effect.
WO2013126146A3 Methods and compositions for enhancing sensitivity of cytotoxic drugs with timely combinatorial therapy with carboxyamidotriazole orotate This invention relates to enhancing sensitivity of cytotoxic drugs by targeting theit interfering mechanisms induced in the tumor microenvironment which lead to drug resistance, using combinatorial therapy with carboxyamidotriazole orotate. Specific doses of cytotoxic drugs are titrated with carboxyamidotriazole orotate to improve the sensitivity and anticancer activity of cytotoxic drugs.
CN103070836A Ciclesonide nanometer freeze-dried powder and preparation method thereof The invention relates to ciclesonide nanometer freeze-dried powder and a preparation method thereof and belongs to the technical field of medicinal preparation. The preparation method comprises the following steps: adding 2400-3900 weight parts of freeze-drying protecting agents into a ciclesonide nanometer grain colloidal solution, dissolving and filtering, and then pre-freezing and freeze-drying, thereby obtaining the ciclesonide freeze-dried powder, wherein the ciclesonide nanometer grain colloidal solution comprises 1 weight part of ciclesonide, 5.0-12 weight parts of carrier materials and 25-35 weight parts of hydrophilic surface active agents. The obtained ciclesonide nanometer freeze-dried powder is excellent in stability and solubility and high in safety and has the advantage of excellent appearance; after re-dissolving, the grain size of the solution is below 800nm and the medicine encapsulation efficiency is above 70%; and the technology provided by the invention has the advantages of simplicity and easiness in operation.
US20050148653 Polymaleimide compounds and their medical use The present invention relates to the use of poly-maleimide derivatives as medicaments. In particular it relates to the use of a maleimide compound of formula (I) or a salt, ester or other physiologically equivalent derivative thereof for use in the manufacture of a medicament for the prophylaxis and/or treatment of a bacterial, viral, fungal or protozoal infection of the reproductive system. The invention further provides such compounds and their use in medicine.
CN101513422A Application of oleanane-28-carboxylic methyl ether-2,11,13(18)-triene in preparing medicament for treating skin diseases The invention discloses application of oleanane-28-carboxylic methyl ether-2,11,13(18)-triene in preparing a medicament for treating skin diseases, and provides a pharmaceutical composition. The pharmaceutical composition is characterized by comprising the oleanane-28-carboxylic methyl ether-2,11,13(18)-triene (I) which is taken as an active component and one or more medicinal accessories. In the pharmaceutical composition provided by the invention, the medicinal accessories are all administrative accessories which are suitable for the skin or mucosa.
EP2266979A1 2-morpholino-4-pyrimidone compounds A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R' represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
CN103599065A 8-methoxypsoralen flexible nanoliposome gel and preparation method thereof The invention relates to 8-methoxypsoralen (MOP) flexible nanoliposome gel and a preparation method thereof. A formula for the gel comprises soybean lecithin, cholesterol, MOP and sodium cholate in a weight ratio of 20 10 3 10. The preparation method comprises the following steps dissolving different drugs in 60 ml of a chloroform-methanol (21) solution according to prescribed proportion and removing the organic solvent via a rotary evaporator through pressure reduction and rotation so as to form a uniform film (A); and heating 5 ml of PBS (10 mmolL) to a temperature of 55 DEG C, pouring the heated PBS into (A) and carrying out stirring in a water bath with a temperature of 55 DEG C for 30 min so as to obtain a transparent uniform milk white liquid. According to the invention, a flexible nanoliposome is used as a drug carrier for MOP, so MOP is allowed to have better penetrability and longer retention time in epidermis and dermis and less MOP enters into blood circulation; thus, the application amount and the application frequency of MOP are reduced, the incidence rate of adverse reaction of MOP is lowered down, and compliance of a patient to treatment is improved.
US20050043355 Immunosuppressive effects of administration of a cyclooxygenase-2 inhibitor and a leukotriene A4 hydrolase inhibitor Treatment with a cyclooxygenase-2 inhibitor and a leukotriene A4 hydrolase inhibitor is described as being useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune diseases.
CN102512386A Amoxicillin or amoxicillin and clavulanate potassium instant chewable tablets for pet and preparation method for same The invention belongs to the field of veterinary medicine, and particularly relates to amoxicillin or amoxicillin and clavulanate potassium instant chewable tablets for pet and a preparation method for the same. The instant chewable tablets are the amoxicillin or amoxicillin and clavulanate potassium instant chewable tablets prepared by combining with orally disintegrating tablets fast in medicine release speed in oral cavity and bad in disintegrating crispness and chewable tablets chewable but slow in disintegrating and medicine release speeds on the basis of the present dosage form of amoxicillin or amoxicillin and clavulanate potassium, so that administration for pet is greatly facilitated, and the antibacterial characteristic of amoxicillin can be adequately exerted. The preparation method for the instant chewable tablets comprises the following steps of: crushing amoxicillin or amoxicillin and clavulanate potassium and related auxiliary materials, and passing through a sieve of 50-100 meshes at first; uniformly mixing the main medicine and the selected auxiliary materials in a proper ratio, and producing wet granules; and drying and straightening the granules, and then tabletting. The instant chewable tablets have broad-spectrum antimicrobial activity and can be used for preventing and treating the bacterial infection of pet. While being used, the preparation is placed in the mouth of pet and fast melted by chewing, so that the convenience and compliance of administration for pet are solved well.
CN103142505A Acetylcysteine composition granules and preparation method thereof The invention belongs to the field of medicament preparations and discloses acetylcysteine composition granules and a preparation method thereof. The acetylcysteine composition granules disclosed by the invention comprise the active ingredients of acetylcysteine, sucrose, steviosin, 95% ethanol and apple essence, and have the advantages of safety, effectiveness, good flowability and stability, accurate dosage, convenience in administration, convenience in carrying, easiness in obtaining raw materials and low cost. The preparation method of the acetylcysteine composition granules disclosed by the invention has the advantages of simplicity in operation, easiness in control and labor-saving and time-saving properties, and is conductive to industrial mass production.
US6911456 Related to organ systems which respond to estrogen agonists or antagonists; in particular, 2-phenyl-3-aroylbenzothiophenes and 1-(alkylaminoethoxy phenyl)-1-phenyl-2-phenylbut-1-enes have wide application as estrogen agonists The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I wherein the variables A, B, Y, D, Z1, G and e are as described herein.
US20080286373 ziprasidone, ziprasidone hcl; mono, di or triglycerides of C12-24 fatty acids, mono, or diesters of c12-c24 fatty acid and polyoxyethylene glycol, vitamin E tocopherol-succinic acid-polyethyleneglycol; sodium lauryl sulfate as anionic surfactant; hydroxyalkylalkyl cellulose; improved bioavailability; A ziprasidone formulation containing at least (a) one ziprasidone compound and at least an excipient component (b) that includes at least one of (i) one or more of a mono-, di-, or tri-ester of C12-24fatty acids and glycerol, in which each fatty acid group is chosen independently of the others, or mixtures thereof; and/or (ii) one or more mono- or di-esters of C12-24fatty acids and polyC2-3alkyleglycol, in which each fatty acid group is chosen independently of the others, or mixtures thereof; and/or (iii) a TPGS (tocopherol-succinic acid-polyethyleneglycol); and where this component (b) may optionally include (iv) optionally free polyC2-3alkyleglycol; (v) optionally free glycerol; and (vi) optionally free fatty acids having 12-24 carbon atoms; and (vii) mixtures thereof; the formulation further comprising (c) at least one surfactant selected from anionic and non-ionionic surfactants and still further comprising (d) at least one hydroxylalkyl alkylcellulose in which each alkyl group and each hydroxyalkyl group independently has from 1 to 4 carbon atoms. The formulation achieves improved dissolution and bioavailability of the formulation. Reduction in side effect profile and increased efficacy and utility in additional indications are also disclosed.
WO2013178745A1 Aqueous-gel-type topical compositions in the form of a homogenous suspension of an active principle of the class of retinoids containing at least one hydrophobic silica The invention relates to aqueous-gel-type topical compositions in the form of a homogenous suspension of an active principle of the class of retinoids containing at least one hydrophobic silica, said active principle preferably having general formula (I), and more specifically 3"-tert-butyl-4'-(2-hydroxy-ethoxy)-4"-pyrrolidin-l-yl-[1,1';3',1"]-terphenyl-4-carboxylic acid. The invention also relates to the preparation mode thereof and to the use of same in the treatment of dermatological conditions.
US7179794 Antibiotics; bactericides Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptoramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.
CN1562075A Use of biological active glass to treat gingivits, cyttarrhagia and odontoseisis syndrom An application of the bioactive glass for preparing toothpaste or solution for treating gingivitis, dental hemorrhage and odontoseisis is disclosed. Said bioactive glass is prepared from SiO2, CaO, Na2O, P2O5 and B2O3.
CN102813670A Application of lycium barbarum polysaccharide in preparing medicine for preventing and treating chronic stress The invention discloses application of lycium barbarum polysaccharide in preparing a medicine for preventing and treating chronic stress. The medicine is characterized in that the extracted lycium barbarum polysaccharide with purity of greater than or equal to 50% is encapsulated or prepared into tablets, wherein each capsule contains 500mg of lycium barbarum polysaccharide, and each tablet contains 500mg of lycium barbarum polysaccharide. The extracted lycium barbarum polysaccharide with purity of greater than or equal to 50% is mixed with corn starch, and then the mixture is encapsulated or prepared into tablets, wherein each capsule contains 500mg of lycium barbarum polysaccharide and 100mg of corn starch, and each tablet contains 500mg of lycium barbarum polysaccharide and 100mg of corn starch. Through the invention, the medicine is a single-formula preparation consisting of lycium barbarum polysaccharide, has an anti-stress effect, can prevent and treat chronic stress disorder, improves the cognitive function, ensures clear efficacy and high safety, and provides a new clinical medication option.
WO2011116123A1 Tafamidis for the treatment of ophthalmic diseases Provided herein are methods of using 2-(3,5-dichlorophenyl)benzo[d]oxazole-6-carboxylic acid (Tafamidis) to treat ophthalmic diseases.
WO2012052562A1 Compositions comprising a filler product and a chemically modified tetracycline The invention relates to a combination product comprising: - a composition A comprising at least one filler product, and - a composition B comprising at least one chemically modified tetracycline, for the treatment of skin aging and scars, compositions A and B being used simultaneously, separately or sequentially over time. The invention also relates to a single pharmaceutical composition or a injectable fixed combination product comprising, in the same physiologically acceptable medium, at least one filler product and at least one chemically modified tetracycline.
CA2662538A1 Azabicyclic compounds as inhibitors of monoamines reuptake The present invention relates to novel compounds of formula (I)´, pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is a group A, K or W wherein A is (II) K is an .alpha. or .beta. naphthyl group, optionally substituted by 1 or 2 groups R18, each of them being the same or different; and W is (III) and wherein G is a 5,6-membered monocyclic heteroaryl, or a 8- to 11-membered heteroaryl bicyclic group; such G may be substituted by (R15)p, which can be the same or different; p is an integer from 0 to 5; R3 is selected in the group consisting of: hydrogen, fluorine, and C1-4alkyl; or corresponds to a group X or X1; R4 is selected in the group consisting of: hydrogen, fluorine, and C1-4alkyl; or corresponds to a group X or X1; R5 is hydrogen or C1-4alkyl; R7 is hydrogen or C1-4alkyl; or is a group X, X1, X2 or X3; wherein X is (IV) X1 is (V) X2 is (VI) and X3 is (VII) R6 is hydrogen or C1-4alkyl; or is a group X or X1; R9 is C1-4alkyl; R10 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents selected from a group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R11 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4aIkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R12 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4aIkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R13 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R14 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4aIkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R15 is selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R16 is hydrogen, C1-4alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-3alkyl; R17 is hydrogen or C1-4alkyl; R18 is selected from a group consisting of: halog
CN103520093A Moxifloxacin hydrochloride injection and preparation method thereof The invention discloses moxifloxacin hydrochloride injection and a preparation method thereof. The injection adopts glucose as an isoosmotic adjusting agent, wherein the injection contains ammonium acetate and acetic acid; pH of the injection is adjusted to 3.0-4.0 by the acetic acid. According to the invention, stable moxifloxacin hydrochloride injection which is easy for industrial production is prepared and a novel drug-use choice is supplied to a patient not suitable for adopting sodium chloride injection.
CN103012099A Fluorenone compounds and preparation method and application thereof The invention discloses fluorenone compounds and a preparation method and application thereof. According to the structural formulas of the fluorenone compounds, R1 is -H, R2 is -OH, a molecular formula is C19H18O6, and one compound is named as gramniphenol D; and R1 is -OH, R2 is -H, a molecular formula is C19H18O6, and the other compound is named as gramniphenol E. According to the preparation method, the fluorenone compounds are prepared from the raw materials including dried branches, leaves or fruits of arundina graminifolia. The preparation method comprises the steps of extract extraction, organic solvent extraction, silica column chromatography and high pressure liquid chromatography separation of the raw materials. The invention further discloses the application of the fluorenone compounds to preparation of anti-AIDS medicines. The gramniphenol D and the gramniphenol E are first detected natural fluorenone replaced by 2-hydroxy-3-methylbut-3-enyloxy. According to cytotoxicity detection on C8166 host cells and inhibition tests on an HIV-1IIIB-induced cytopathic effect (CPE) of the C8166, the two fluorenone compounds have good anti-HIV-1 activity, the EC50 values of the two fluorenone compounds are respectively 1.46+/-0.15 microgram/mL and 1.58+/-0.20 microgram/mL, and the therapeutic index (IT) values of the two fluorenone compounds are respectively 137 and 126.6. The fluorenone compounds have novel structures and high activity, and can serve as guiding compounds of the anti-AIDS medicines.
US7160894 Antagonist of phosphorylation of myosin regulatory light chain, enzyme inhibitors; therapeutic treatment of glaucoma, bronchial asthma, chronic obstructive pulmonary disease, nervous system disorders; 4-(2,3-dihydro-1,5-diazaphenalen-1-yl)cyclohexylamine A novel compound represented by the formula (1): [R1 represents hydrogen atom, chlorine atom, or hydroxyl group; X1 . . . X2 represents—CH(R2)—CH(R3)—, —CH(R2)—CH(R3)—CH(R4)—, etc.; R2 to R4represent hydrogen atom, or an alkyl group; A1, A11, A2, and A21 represent hydrogen atom, or an alkyl group; Y represents —CH(A3)—, —CH(A3)—C(A4)(A41)—, —CH(A3)—C(A4)(A41)—C(A5)(A51)—, or a single bond; A3, A4, A41, A5, and A51 represent hydrogen atom, or an alkyl group; Z represents hydroxyl group, or —N(A6)(A61); A6 represents hydrogen atom, or an alkyl group, A61 represents hydrogen atom, an alkyl group, an aralkyl group, etc.; and groups in each of one or more combinations selected from the group consisting of combinations of A6 and A3, A6 and A4, A6 and A1, A6 and A2, A2 and A3, A2 and A4, A6 and A5, A3 and A1, and A5 and A1 may bind to each other to form a 5- or 6-membered ring], or a salt thereof, which potently inhibits the phosphorylation of myosin regulatory light chain.
WO2010110223A1 Fucoidan having antitumor activity Disclosed is a medium-molecular weight fucoidan which can be used in treating and/or preventing proliferative diseases, in particular, cancer. Specifically disclosed are a medium-molecular weight fucoidan, a method for producing the same, a medicinal composition containing the same, and use of the medium-molecular weight fucoidan in producing a drug for treating and/or preventing preventing proliferative diseases, in particular, cancer. The aforesaid medium-molecular weight fucoidan has an average molecular weight of about 6,000 to about 2,000,000, preferably an average molecular weight of about 40,000 to about 330,000, more preferably an average molecular weight of about 40,000 to about 244,000, and still more preferably an average molecular weight of about 80,000 to about 200,000.
CN101317858B Exogenous injury ulcer treating medicine The present invention relates to traumata ulcer ingot, which is produced with the following raw materials in weight proportions: 10 to 20 proportions of pearl, 5 to 10 proportions of calomel and 5 to 10 proportions of borneol. The pearl particles are firstly put into a closed vessel, which is then baked over a fire. The closed vessel is shaken continuously during the bake process. The closed vessel is taken from the fire and natural cooling is performed. The pearl particles become baked pearl; various raw materials are mixed and ground. The product can be obtained by filtering the mixture with a screen with a filtering size ranging from 100 to 150 meshes. The present invention has the remarkable advantages that: 'platinum ingot' produced by adopting the method provided by the present invention has rapid and strong detumescence, acesodyne and ulcer elimination effect in curing skin infect and ulcer. The 'platinum ingot' can quickly alleviate anguish of sufferer with a cure rate reaching 100 percent.
US20130059016 Clay compositions The present invention relates to liquid or semi-solid pharmaceutical compositions, more specifically to aqueous pharmaceutical suspension or semi-solid paste containing natural mineral clays as active ingredients. These compositions are particularly useful for the treatment of acute and chronic diarrhea.
EP1827408A1 Method for treating skin disorders with xanthophylls The present invention provides for a method for treating a skin disorder in a mammal inflicted with a skin disorder. The present invention also provides for a method for retarding or reversing the loss of collagen fibers, abnormal changes in elastic fibers, or deterioration of small blood vessels in sundamaged mammalian skin. The present invention also provides for a method for exfoliating the skin surface of a mammal. The present invention also provides for a method for treating or preventing acne or a pimple in a mammal in need thereof. The methods include topically administering, to a mammal in need of such treatment, a composition that includes xanthophylls in a nontoxic amount, effective to treat the skin disorder.
WO2010094986A1 Micronized carotenoid preparation as immunostimulant for crustaceans The present invention refers to micronized carotenoids in an oily carrier; the composition acts as immunostimulant for crustaceans.
WO2006098834A8 Crystalline forms of ziprasidone mesylate Provided are polymorphic forms of ziprasidone mesylate and processes for their preparation.
EP0959878B1 Method for treating renal failure Methods of controlling phosphate metabolism and metabolic acidosis in patients suffering from renal failure and associated hyperphosphatemia or patients predisposed to development of a hyperphosphatemic condition are provided. The method in accordance with this invention comprises administering to a patient a ferric-containing compound selected from the group consisting of ferric citrate, ferric acetate, and combinations thereof. Therapeutic benefit can be realized in accordance with such method by administering the compound orally to a patient to contact and bind with ingested phosphate in the patient's digestive tract, and thereby prevent its intestinal absorption.
CA2613647A1 Self-sterilizing products comprising a polymer bound to a phthalocyanine derivative Self-sterilising products, and in particular novel products comprising phthaloeyanine derivatives bound to polymers, a process for the preparation of said products and their use for preparing self-sterilising industrial and medical articles or devices, are described.
WO2014052583A1 Compounds for the treatment of obesity and methods of use thereof Pentacyclic triterpene weight loss agents are provided herein. Also provided are pharmaceutical formulations containing a therapeutically effective amount of one or more of the weight loss agents, or pharmaceutically acceptable salts or prodrugs thereof, in combination with one or more pharmaceutically acceptable excipients. The pharmaceutical formulations can be administered to a pre-obese, obese, or morbidly obese patient to induce weight loss, reduce body fat, reduce food intake, improve glucose homeostasis, prevent obesity, or a combination thereof. The weight loss agents can also be co-administered with leptin or a leptin analog.
CN102716117A Application of naringenin in preparing medicines for resisting apoptosis of retinal photoreceptor cell The invention relates to a flavonoid organic effective component-containing medicinal preparation, in particular to the application of naringenin in preparing medicines for resisting apoptosis of a retinal photoreceptor cell. According to the application, the compound naringenin embodying the uses has a protective action on the photochemical damage of the retinal photoreceptor cell, can be used for resisting the apoptosis of the retinal photoreceptor cell and can be used for preparing various medicines for resisting the apoptosis of the retinal photoreceptor cell so as to be in favor of increasing the life quality of human.
CN103097393A Quinoxaline compound [Problem] To provide a compound that has the effect of inhibiting PDE9 and is useful as an active ingredient in a therapeutic and/or prophylactic agent for urine collection disorders, urination disorders, diseases of the bladder and urinary system, and the like. [Solution] Investigating compounds that have the effect of inhibiting PDE9 and are useful as active ingredients in a therapeutic and/or prophylactic agent for urine collection disorders, urination disorders, diseases of the bladder and urinary system, and the like, the inventors of the present invention verified that an imidazoquinoxaline compound or a triazolo-quinoxaline compound has the effect of inhibiting PDE9, thereby completing the present invention. This imidazoquinoxaline compound or triazolo-quinoxaline compound has the effect of inhibiting PDE9 and can be used a therapeutic and/or prophylactic agent for urine collection disorders, urination disorders, diseases of the bladder and urinary system, and the like.
WO2013177608A1 Method of treating scedosporium spp. infection The present invention provides a method of treatment of Scedosporium spp. infection in an animal comprising the step of administering to the infected animal an effective amount of a compound of formula I or a pharmaceutically-acceptable salt thereof
US20050239694 Cyclic depsipeptide as chemotherapeutic anticancer agent Serratamolide, also named cyclo[(3R)-3-hydroxydecanoyl-L-seryl-(3R)-3-hydroxydecanoyl-L-seryl], is a cyclic depsipeptide isolated from cultures of bacteria of the species Serratia marcescens. Serratamolide decreases the viability of, and induces apoptosis in several cancer cells (leukemias, myelomas, carcinomas, etc.), virtually with no effect on non-cancer cells. This makes serratamolide, and its pharmaceutically acceptable addition salts and/or solvates, useful as anticancer chemotherapeutic agent, particularly against leukemia, lymphoma, myeloma, carcinoma, melanoma and sarcoma.
CN102579397A Preparation method for vitamin A microcapsules Disclosed is a preparation method for vitamin A microcapsules. The method includes feeding silicone oil of low viscosity in a reaction kettle with a temperature control stirring function; dispersing vitamin A in water solution of gelatin, Arabic gum and maltodextrin through a homogenizer, stirring at a normal temperature and at a low speed of 80-250 revolutions per minute (rpm), adding the generated suspension dropwisely and slowly to the reaction kettle through a micro hole, adding about 1% of formaldehyde solution, cooling the reaction kettle to a temperature below 5 DEG C, keeping stirringfor 2-8 hours, and globular solids with silicone oil are generated; subjecting the globular solids with the silicone oil to a cold drying in dry air under the normal temperature of 40 DEG C until themoisture content is lower than 8%, washing collected dry globules with suitable organic solvents so as to eliminate the silicone oil on the surface, subjecting the globules to a vacuum drying under atemperature of 30 DEG C to 50 DEG C so as to obtain semi-finished products of the vitamin A microcapsules; and screening the semi-finished products of the vitamin A microcapsules to obtain finished products. The preparation method for the vitamin A microcapsules has the advantages that the production cost is low, the operation is simple, the finished products are complete globules with a particlesize distribution of 40-200 meshes and have a good fluidity; and the yield is high because almost no active substance loss exists during the process implementation.
CN101084944B Composition for prophylaxis or treatment of urinary system infection The present invention relates to a composition for prophylaxis or treatment of urinary system infection, comprising a matrix metalloproteinase inhibitor.
US7517902 1-[4-(3-amino-7-fluoro-1H-indazol-6-yl)phenyl]-3-(2-fluoro-5-trifluoromethyl-phenyl)urea; protein kinases (Vascular Endothelial Growth Factor Receptor 2 and Tie-2), inhibitor; anticarcinogenic, antiinflammatory agent; neovascularization, lung and breast cancer, rheumatoid arthritis Disclosed are novel substituted indazole compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising such compounds.
WO2006025431A1 Antagonist against tolerance to anticancer drugs An ABC transporter protein expression inhibitor comprising, as the active ingredient(s), 0.001 to 100 nM of one or more members selected from among steroid hormones, compounds having a female hormone function, analogous compounds thereof and antagonistic inhibitors therefor; an anticancer composition containing this ABC transporter protein expression inhibitor and an anticancer drug; and cells useful in developing an anticancer drug. Thus, a drug which inhibits the expression of an ABC transporter to thereby overcome tolerance to anticancer drugs; cancer cells useful in screening this drug; and an anticancer drug efficacious even against such a cancer as having acquired tolerance to anticancer drugs are provided.
US20100040679 Compositions for Reducing Nicotine Withdrawal Symptoms and/or Tobacco Usage Compositions useful for treating an individual with nicotine dependence comprising a combination of an α3β4 nicotinic receptor antagonist and a nicotine metabolite are disclosed. More particularly, compositions comprising cotinine or a pharmaceutically acceptable salt thereof are disclosed. Methods of alleviating nicotine withdrawal symptoms and/or tobacco usage by administration of these compositions are also disclosed.
US20110207769 Stable crystalline salt of (r)-3-fluorophenyl-3,4,5-trifluorobenzylcarbamic acid 1-azabicyclo [2.2.2]oct-3-yl ester The present invention refers to a stable crystalline salt of (R)-3-fluorophenyl-3,4,5-trifluorobenzylcarbamic acid 1-azabicyclo[2.2.2]oct-3-yl ester and its use as medicament, in particular for the treatment of urinary incontinence or other diseases involving genitourinary disorders
CN102872132A Application of Houttuynoid D in anti-helicobacter pylori drug An activity experiment in vitro indicates that Houttuynoid D has strong anti-HP (Helicobacter Pylori) activity. Houttuynoid D can be used for treating diseases such as acute and chronic gastricism, gastric ulcer, duodenal ulcer and the like and applied to preparing drugs for treating acute and chronic gastricism, gastric ulcer and duodenal ulcer. The use of Houttuynoid D in preparing the anti-helicobacter pylori drug involved in the invention is disclosed for the first time; as the framework type of Houttuynoid D is a brand new framework type and Houttuynoid D has an unexpectedly high inhibition activity for the helicobacter pylori without possibility of giving any implication by other compounds, Houttuynoid D has outstanding substantive features; and simultaneously, the application of Houttuynoid D for preventing and treating the helicobacter pylori apparently has obvious progress.
US20090110745 Over-the-counter vitamin/nutriceutical formulation that provides neuroprotection and maintains or improves cognitive performance in alzheimer's disease and normal aging The present invention provides methods for improving cognitive function, improving mood, and decreasing aggression in a normal adult subject, and in a subject having symptoms characteristic of a neurological disorder, by administration of a nutriceutical formulation of the invention to the subject. The invention additionally features methods of treating neurological disorders, depression, and aggression using nutriceutical formulations. Nutriceutical compositions and formulations for use in the methods of the invention, and kits containing nutriceutical compositions and formulations, are also provided.
WO2007076086A3 Tricyclic spiro compounds useful as transforming growth factor modulators The invention is related to compounds of formula (I) that can be used as antagonists of the TGFβ family type I receptors, Alk5 and/or Alk4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such as fibrosis (e.g., renal fibrosis, pulmonary fibrosis, and hepatic fibrosis), progressive cancers, or other diseases for which reduction of TGFβ family signaling activity is desirable.
CN102836144A Deoxidized epinephrine oral instant film and preparation method thereof The invention belongs to the technical field of medicine, and relates to a deoxidized epinephrine oral instant film and a preparation method of the deoxidized epinephrine oral instant film. The deoxidized epinephrine oral instant film provided by the invention is good in taste, quick to dissolve in the oral cavity and fast in drug release, and can be taken without drinking water. A preparation technology of the deoxidized epinephrine oral instant film is convenient and feasible, so that the deoxidized epinephrine oral instant film is directly prepared by selecting a proper film forming material, a filler and a sweetener without adding a taste masking agent. The deoxidized epinephrine oral instant film provided by the invention is utilized to eliminate nasal and pharyngeal mucosa hyperemia, relieve nasal mucosa hyperemia and swelling, and alleviate a nasal obstruction symptom caused by cold, influenza, allergic reaction or non-allergic rhinitis, and the like.
CN102499940A Medicine for promoting chickens to grow healthily and quickly The invention discloses a medicine for promoting chickens to grow healthily and quickly. A method for preparing the medicine comprises the following steps of: mixing 1 to 3 weight parts of vitamin B1, 1 to 3 weight parts of vitamin B2, 1 to 3 weight parts of vitamin B6, 1 to 3 weight parts of vitamin B12, 1 to 5 weight parts of nicotinamide, 1 to 5 weight parts of calcium pantothenate and 1 to 15 weight parts of astragalus polysaccharide, dissolving in distilled water or water for injection to obtain an aqueous solution; mixing the aqueous solution, and an aqueous solution obtained by diluting 30 to 80 weight parts of oligomeric syrup by using the distilled water or the water for injection, and filtering, wherein the relative density of the mixed solution is between 1.0 and 1.05; and sterilizing to prepare brown liquid. The medicine has the characteristic of reducing a chicken feed conversion rate obviously, along with convenience for taking and can be used for promoting the chickens to grow healthily and quickly.
US6911468 Useful as a prophylactic or therapeutic agent for diabetes or the like A compound of the formula (I): wherein X1 and X2 are the same or different and each is a bond or a spacer having 1 to 20 atom(s) in the main chain; one of R1 and R2 is a cycle group having substituent(s) selected from 1) an optionally substituted carboxy-C1-6 alkoxy group and 2) an optionally substituted carboxy-C1-6 aliphatic hydrocarbon group, wherein the cycle group optionally has additional substituent(s), and the other is an optionally substituted cycle group or a hydrogen atom; and R3, R4 and R5 are the same or different and each is a hydrogen atom or a substituent, or R4 may link together with R3 or R5 to form an optionally substituted ring; provided that when R3 is a hydrogen atom, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-cyclohexylphenyl; when R3 is 4-methoxyphenyl, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-methoxyphenyl; and when R1 or R2 is a hydrogen atom, the adjacent X1 or X2 is not a C1-7 alkylene; or a salt thereof exhibits a protein tyrosine phosphatase inhibitory action and is useful as a prophylactic or therapeutic agent for diabetes or the like.
US20110201611 Process for the Preparation of Compositions for Modulating a Kinase Cascade and Methods of Use Thereof The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention.
US20110224239 Combinations Comprising a S1P Receptor Agonist and a JAK3 Kinase Inhibitor The invention provides a pharmaceutical combination comprising: a) at least one S1P receptor agonist, and b) at least one JAK3 kinase inhibitor and a method for treating or preventing autoimmune diseases or cell, tissue or organ graft rejection using such a combination.
US7232813 Neutral endopeptidase (NEP) and human soluble endopeptidase (hSEP) inhibitors for prophylaxis and treatment of neuro-degenerative disorders The invention relates to a novel use of known benzazepine, benzoxazepine, benzo-thiazepine-N-acetic acid and phosphono-substituted benzazepinone derivatives having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity. The compounds of the invention are useful for the preparation of pharmaceutical compositions for prophylaxis and treatment of neurodegenerative disorders. The compounds of the invention are known from the European patents EP 0 733 642 and EP 0 916 679, and can be described by the general formulae (1): wherein the symbols have the meanings as given above in the description.
CN102488905A Electric and magnetic conductive gamma-iron oxide/polyaniline-mesna nanoparticles and preparation method thereof The invention relates to electric and magnetic conductive gamma-iron oxide/polyaniline-mesna nanoparticles and a preparation method thereof. The method comprises the following steps of: mixing aniline and a hydrochloric acid solution, adding gamma-iron oxide, stirring, adding ammonium persulfate, and stirring, wherein the molar ratio of the ammonium persulfate to the aniline is not less than 1:1; washing, drying in vacuum, soaking in ethanol and acetone, performing suction filtering, drying, dedoping polyaniline by using ammonia water to obtain eigen polyaniline, washing by using water, and drying in vacuum to obtain a dedoped product gamma-iron oxide/polyaniline; and adding the gamma-iron oxide/polyaniline and mesna in different mass ratios into various protonic acid solutions with the concentration of more than 0.1 mol.L<-1>, stirring, performing suction filtering in vacuum under reduced pressure, washing by using water and ethanol until filtrate is colorless, and drying in vacuum to obtain a product gamma-iron oxide/polyaniline-mesna. The defects that an effective treatment group of a medicine is influenced due to fixation, is limited by release dynamics, and the like are overcome; and the nanoparticles have the characteristics of a targeted medicine and are applied to the targeted treatment of human body diseases, and the method is simple, convenient and economic.
CN1569119A Dogwood extraction and its preparation method and usage The invention provides a dogwood extraction and its preparation method and use thereof, wherein the preparation consists of extracting dogwood with alcohol, depression concentrating the raffinate to a finite density, collecting the deposition, decompressing and drying, obtaining extract A, passing through macroscopic adsorption resin column, removing foreign substance through washing, ethanol elution, collecting the eluent, decompressing and drying, obtaining extract B, mixing extract A and B homogeneously, thus obtaining the dogwood extract. The invention discloses its novel pharmaceutical use in preparing medicament for prevention and treatment of diabetic blood vessel pathological changes and for reducing blood sugar.
WO2014017593A1 Adhesive patch and production method therefor A production method for an adhesive patch comprising a supporting body layer and an adhesive layer, said production method including: a mixture preparation step in which asenapine or a pharmacologically acceptable salt thereof and a sodium acetate having a cumulative volume of 50% in the particle size distribution and a particle diameter (D50) of 40-1,000 µm are mixed such that the particle diameter (D50) of the sodium acetate and sodium diacetate generated from the sodium acetate is no more than 10 µm, and a mixture containing the sodium diacetate and the asenapine or a pharmacologically acceptable salt thereof is obtained; and an adhesive layer forming step in which an adhesive layer composition obtained by mixing the mixture and a pressure-sensitive adhesive base is used and the adhesive layer is formed, said adhesive layer containing the sodium diacetate, asenapine or a pharmacologically acceptable salt thereof, and the pressure-sensitive adhesive base.
CN101919864A Tolvaptan medicinal composition and preparation method thereof The invention relates to a tolvaptan medicinal composition and a preparation method thereof. 1,000 tablets of the composition consist of 15 to 60 grams of tolvaptan, 15 to 60 grams of hydroxypropyl-beta-cyclodextrin, 30 to 120 grams of microcrystalline cellulose with pH of 102, 10 to 40 grams of cross-linked polyvinylpyrrolidone, 10 to 40 grams of pregelatinized starch, 20 to 80 grams of lactose and 1 to 10 grams of magnesium stearate. In the preparation method, the conventional preparation technology is adopted after the tolvaptan and the hydroxypropyl-beta-cyclodextrin are subjected to special processing. The prepared tolvaptan medicinal composition has the advantages of high fluidity, high dissolution, small tablet weight variation, high stability, high biological utilization degree and good therapeutic effect.
CN1634069A Calcium, zinc and ferrum composite oral liquor and its preparing process The invention provides a calcium, zinc and ferrum composite oral liquor and its preparing process, wherein the oral liquid comprises the constituents of (by weight percent) soluble calcium agent 2-8 parts, soluble ferrum agent 0.5-3 parts, soluble zinc agent 0.1-0.6 part, vitamin B2 0.01-0.06 part, water by the weight ratio of 100 : 2-12. The process for preparation comprises the steps of heating, stirring, mixing, cooling down, secondary filtering, loading and sterilizing.
US20080193444 Methods of suppressing LTP inhibition Methods and compositions for suppressing amyloid-mediated inhibition of long-term potentiation (LTP) are provided.
US20110033466 Human transcriptomes Global gene expression patterns have been characterized in normal and cancerous human cells using serial analysis of gene expression (SAGE). Cancer cell-specific, cell-type specific, and ubiquitously expressed genes have been identified. This information can be used to provide combinations of cell type- and cancer-specific gene probes, as well as methods of using these probes to identify particular cell types, screen for useful drugs, reduce cancer-specific gene expression, standardize gene expression, and restore function to a diseased cell or tissue.
US20110244034 Sustained release drug delivery system The invention discloses a controlled release dosage form comprising a therapeutically effective amount of a pharmaceutically active agent, illustrated by Acyclovir, that would release in about 12 hours not more than about 90% of the said active agent in a simulated gastric juice in a first order rate of release in a USP type 1 dissolution test, and not containing a solubilizer or a swelling enhancer or both, comprising (a) a tablet made from polymer matrix of at least two biocompatible polymers, illustrated by Carbopol 974P and polyethylene oxide, the said pharmaceutically active agent and pharmaceutically permitted excipients; the said tablet capable of rapid swelling without disintegration in the said simulated gastric juice to a size that shall result in its gastric retention in the stomach and start controlled release of the said active agent by starting controlled erosion as well as diffusion immediately after coming into contact with the said gastric juice, or (b) microspheres of ungrafted chitosan or a chitosan derivative illustrated by thiolated chitosan and trimethyl chitosan, or Carbopol incorporating the said active agent, wherein the said pharmaceutically active agent is not a polymeric molecule and after administration in stomach, the said microspheres adhare to the gastric mucosa for a long time releasing the active agent in a controlled way.
CN101327219A Prednisolone acetate in situ forming eye gel The invention discloses an instant prednisolone acetate eye gel and a preparation method thereof. According to the invention, 1000ml of the instant prednisolone acetate eye gel contains 1g to 20g of prednisolone acetate, 0.05g to 1g of preservative, 1.0g to 7.5g of osmotic pressure adjusting agent, and 30g to 150g of gel stroma, and the rest includes acid-alkali buffer and water for injection. The invention, through the optimization of accessories and the improvement of the technique, enriches the pharmaceutical dosage form of the prednisolone acetate, greatly prolongs the time for which the medicine stays in the eyes, and not only improves the curative effect but also can reduce the times for which the medicine is dropped into the eyes so as to prevent the development of cataracts and glaucoma. Besides, the fluidity of the instant eye gel is low so that the medicine absorption of the lacrimal passages and the rhinopharynx mucous membranes so as to reduce the side effect suffered by the whole body.
EP1284734B1 Isoquinoline derivatives as protein kinase inhibitors Novel isoquinoline derivatives which are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes are disclosed. Preferred compounds which are specific inhibitors of protein kinase B are also disclosed. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune disease, are disclosed.
CN1813971A Effervescent tablet for treating infant diarrhea The present invention provides a Xiesuting effervescent tablet for effectively curing diarrhea in child. It is made up by using 720g of humifuse euphorbia, 108 g of cutch, 120 g mume fruit, 180 g of stir-fried crataegus fruit, 360 g of poria, 180 g white peony root, 720 g of licorice and 150 g of lactose, 278 g of sodium hydrogen carbonate, 222 g of citric acid, 50 g of aspartame, 50 g of polyethylene glycol 6000 and 2 g of magnesium stearate through a certain preparation process.
WO2012029836A1 Method for producing 1-triazole-2-butanol derivative The purpose of the invention is to provide a method for producing a compound of formula (1) with high yield through a ring-opening addition reaction of an amine with epoxytriazole under mild conditions without using a large excess amount of 4-methylenepiperidine. The method is a method for producing (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol or an acid addition salt thereof, and comprises reacting (2R,3S)-2-(2,4-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]oxirane with an acid addition salt of 4-methylenepiperidine in a reaction solvent in the presence of a hydroxide of an alkali metal or an alkaline earth metal selected from the group consisting of lithium, sodium, calcium, and strontium, or a hydrate thereof.
WO2010000404A1 Oxazolidinones for the treatment of inflammatory conditions of the gastrointestinal tract The present invention relates to the use of selective inhibitors of coagulation factor Xa, in particular of oxazolidinones of the formula (I), for the treatment and/or prophylaxis of inflammatory conditions of the gastrointestinal tract such as inflammatory bowel disease (IBD) and celiac disease and/or disorders related to inflammatory bowel disease (IBD) and/or celiac disease such as thromboembolic events (including e.g. pulmonary embolism (PE), arterial and venous thrombosis, myocardial infarction, stroke) as well as their use for the preparation of pharmaceutical drugs for the treatment and/or prophylaxis of inflammatory bowel disease (IBD) and/or celiac disease and/or disorders related to inflammatory bowel disease (IBD) and/or celiac disease such as thromboembolic events.
US20100056555 Method of treating ras associated cancer New methods of treating Ras associated cancer, and especially for treating cancer that is resistant or refractory to other treatment methods, including resistant or refractory to treatment with C225 and/or CPT-11, are provided. The new methods employ PEG-conjugated 7-ethyl-10-hydroxycampothecin, alone, or in combination with other art-known anticancer agents or modalities.
US7148208 For therapy and prophylaxis S-alkylsiothiouronium derivatives such as S-ethylisothiouronium diethylphosphate are used for the treatment of headaches, in particular, migraines, as well as for the prevention or treatment of nausea and vomiting. The compositions of the invention are also effective in preventing or alleviating emesis associated with migraines or other medical conditions such as chemotherapy or radiotherapy, as well as other symptoms of migraines including phonophobia and photophobia.
US7161031 Amino-substituted sulfonanilides and derivatives thereof for treating proliferative disorders Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: Ar, X, X1, g, R and R3 are as defined herein.
CN101791319B Female pudendum nursing product The invention relates to a female pudendum nursing product, which consists of germicidal effervescent tablets and nutrient clean nursing liquid, wherein the germicidal components of the germicidal effervescent tablets contain sodium chlorite. Because the disinfection is separated from cleaning and nursing, the compound female pudendum nursing product can really play respective role; and because chlorine dioxide is introduced into the pudendum cleaning system in a form of effervescent tablet cleaning liquid, the guarantee period is prolonged and use concentration of the chlorine dioxide is increased, and the problems that the chlorine dioxide has poor chemical stability and cannot be kept for a long term are solved.
US20120308633 Nanostructured material formulated with bone cement for effective antibiotic delivery This invention uses mesoporous silica nanoparticles and other nanostructured materials to formulate polyacrylate-based bone cement for achieving an enhanced and controlled elution of active ingredients such as antibiotics. This invention overcomes the limitation of low antibiotic release from commercial polyacrylate-based bone cements using for example, PMMA. In certain aspects, the formulation enables a sustained release of antibiotics from the bone cement over a period of 80 days and achieves 70% of total drug release, whereas the commercial antibiotic bone cement (e.g., SmartSet GHV) only releases about 5% of the antibiotics on the first day and subsequently an almost negligible amount. In addition, the mechanical properties of our formulated bone cements are well retained. The inventive bone cement exhibits good antibacterial properties and has very low cytotoxicity to mouse fibroblast cells.
CN102755620A Appetizing health care product used for hepatitis B patients The invention relates to an appetizing health care product used for hepatitis B patients. The health care product is prepared by the following raw materials: subprostrate sophora, codonopsis pilosula, rhizoma atractylodis macrocephalae, turtle shell, agilawood, costus root, radix curcumae, radix bupleuri, rheum officinale, akebiaquinata, plantain seed, angelica sinensis, soapstone, desmodium, Chinese violet, liquorice, rhizoma corydalis, elecampane, amomum kravanh, fructus amomi, ginger, fructus ligustri lucidi, grifola, poria and aspongopus. The health care product can effectively control clinical symptoms of gastric ulcer of midsection ache, belching, sour regurgitation, regurgitation and the like, and big and small three yang into yin of hepatitis B and the liver function can be restored.
EP1879570A2 Inhibition of reactive oxygen species and protection of mammalian cells Methods and compositions useful for neuronal protection in retinal cells in vitro and the protection of mammalian cells from reactive oxygen species in vivo are provided. UltrafÊne nano-size cerium oxide particles, less than 10 nanometers in diameter, have been provided to decrease reactive oxygen species (ROS) in retina tissue that generates large amounts of ROS. These reactive oxygen species (ROS) are involved in light- induced retina degeneration and age-related macular degeneration (AMD). Cerium oxide nanoparticles have been used to promote the lifespan of retinal neurons and protect the neurons from apoptosis induced by hydrogen peroxide in vitro and in vivo. The neuronal protection in retinal cells is achieved by decreasing generation of intracellular reactive oxygen species (ROS). Thus, cerium oxide particles are used to promote the longevity of retinal neurons in vitro and mammalian cells in vivo.
CN101708158A Eriocalyxin B nanosuspension and preparation method thereof The invention discloses eriocalyxin B nanosuspension and a preparation method thereof. The eriocalyxin B nanosuspension is characterized by comprising a therapeutic effective dose of eriocalyxin B nano-suspension anhydrous substance and water or other injectable solution; and the eriocalyxin B nanosuspension anhydrous substance comprises eriocalyxin B, surface active agent, additive and an dryingsupporting agent, wherein the weight ratio of the eriocalyxin B to the surface active agent is 1:0.05-1:5. In the invention, the problem of the solubility of the eriocalyxin B is solved, the preparedagent can be free of organic solvent, and the dose of the surface active agent is small; moreover the nanosuspension can also change the distribution of the medicament in vivo and reduce toxic and side effect; and the prepared nanosuspension anhydrous substance has favorable stability.
EP1043021B1 Purine derivatives for the treatment of allergic diseases and systemic lupus erythematosus Type 2 helper T cell-selective immune response suppressors, immune response modulators and antiallergic agents containing purine derivatives represented by general formula (I) as the active ingredient wherein R2 represents H or hydrocarbyl; R6 represents amino mono- or disubstituted by OH, NH¿2? or hydrocarbyl; R?8¿ represents OH, SH, acyloxy or hydrocarbyloxycarbonyloxy; and R9 represents hydrocarbyl, provided that in the hydrocarbyl represented by R?2 and R9, -CH¿2- not directly bonded to the purine skeleton may be replaced by CO, SO2, O or S and C-H not directly bonded to the purine skeleton may be replaced by N, C-halogeno or C-CN.
EP1461316B1 Synthesis of 2-cyanoziridine-1-carboxamide The present invention provides a process for producing an aziridine-1-carboxamide of the formula: (I) from an aziridine of the formula: (II) and an isocyanate of the formula R5-N=C=O, where R?1, R2, R3, R4 and R5¿ are those defined herein. In addition, the present invention also provides a process for producing a 4-imino-1,3-diazabicyclo[3.1.0]-hexan-2-one of the formula: (a) from the aziridine-1-carboxamide of Formula (I).
US8501737 Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase This invention comprises the novel compounds of formula (I) wherein t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
WO2013148864A1 Curaxins for use in treating breast cancer and method for identifying patients likely to respond The present invention relates to the treatment of breast cancer which is estrogen receptor positive (ER+) and/or human epidermal growth factor receptor 2 positive (HER2) and/or progesterone receptor positive (PR) and/or facilitates chromatin transcription positive (FACT +) with a curaxin, including curaxin 137. The presen invention also pertains to a method of identifying a subject who has a breast cancer tumor and is likely to respond to treatment with a curaxin.
EP1231910B1 Pentamidine for treating cancer The present invention relates to the treatment of cancer with compounds that inhibit the activity of endo-exonuclease. Endo-exonuclease has been shown to be necessary for the repair of damaged DNA. Compounds that inhibit the activity of endo-exonuclease have been shown to be particularly effective for treating cancer when used in combination with drugs that induce DNA breaks such as cisplatin and mitomycin C. These compounds have a synergistic effect when used in combination for inhibiting tumour growth. The invention includes pharmaceutical compositions for inhibiting tumour growth comprising a compound that inhibits endo-exonuclease activity. These pharmaceutical compositions preferably include compounds that induce DNA breaks. The invention includes methods of treating cancer with these pharmaceutical compositions and uses of these compositions to treat cancer. The preferred compounds that inhibit the activity of endo-exonuclease have low toxicity. One such compound is pentamidine. The invention also includes a method for diagnosing cancer and monitoring its progression. This aspect of the invention involves isolating serum from a patient; measuring the concentration of endo-exonuclease in said serum and determining whether said concentration is above a predetermined mean.
US20100104661 Discontinuous methods of treating cancer Disclosed are methods of treating taxane sensitive tumors (i.e., cancers treatable with taxanes) using a taxane and the discontinuous dosing of lonafarnib.
CN103040793A Cefaclor oral instant film preparation and preparation method thereof The invention discloses a cefaclor oral instant film and a preparation method thereof. The instant film comprises a main drug of an effective dose of a drug and auxiliary materials, wherein the main drug is cefaclor, and the auxiliary materials include a water-soluble polymer, a plasticizing agent, a taste masking agent and an edible colourant. The preparation method comprises the steps of mixing the main drug cefaclor, the taste masking agent and anion exchange resin into water to form uniform dispersion liquid, filtering and removing moisture to prepare a cefaclor/anion exchange resin compound, dispersing the compound and other auxiliary materials into the water to prepare a stable dispersion solution, adopting a solution coating method, using a coater to coat the dispersion solution on a polyester stripping film or a release paper surface to form the film, drying in an airblast oven at 50 DEG C-80 DEG C, and cutting the drug film into a specific size. The instant film can be dissolved in an oral cavity within 5-60 seconds, so that the bioavailability of the cefaclor, namely an effective drug ingredient, is improved greatly, and an effect is exerted quickly.
CN102008448A Metadoxine granules and preparation and quality control method thereof The invention discloses metadoxine soluble granules as well as a preparation method and a quality control method thereof. The granules comprise the following raw and auxiliary materials in parts by weight: 250-500 parts of metadoxine and 350-550 parts of maltodextrin. The granules in the invention have the advantage of stability proved by an accelerated test, in which the granules are kept in an condition with the relative humidity of 75%+/-5% at 40+/-2 DEG C for 6 months, and a long-tem test, in which the granules are kept in a thermostat with the relative humidity of 60%+/-10% and the temperature of 25+/-2 DEG C for 12 months. A compliance test of the granules indicates the non-compliance rate of the granules in a test group is 3%, and the non-compliance rate of the granules in a control group is 23%. The result of a compatibility test of the granules indicates that the metadoxine soluble granules have no interaction with auxiliary materials in a prescription.
US8202867 Methods of using hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide Disclosed are hydrates and polymorphs of 4- [[(7R)-8-cyclopentyl-7 -ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide: as well as, processes for preparing them and their use as pharmaceutical compositions with antiproliferative activity.
CN103316035A Use of sodium bicarbonate in preparation of medicines for treating cancer The invention provides a use of sodium bicarbonate in preparation of medicines for treating cancer. The molecular formula of sodium bicarbonate is NaHCO3. Researches verify that sodium bicarbonate induces neoplasm necrosis or inhibit tumor growth, has the effect of inhibiting tumor angiogenesis and can be used to prepare medicines for tumor transarterial embolization and tumor transarterial chemoembolization, especially medicines for artery chemoembolization of liver cancer. Researches show that the curative effect of sodium bicarbonate combined in use with tumor transarterial chemoembolization or tumor transarterial embolization is remarkably greater than single use of sodium bicarbonate or tumor transarterial chemoembolization or tumor transarterial embolization. The dosing form of the medicine is injection. The invention develops novel use of sodium bicarbonate in preparation of medicines for treating cancer, the medicine is a medicine which is delivered to the tumor body and is free from toxicity to human body, and the treatment price can be lowered.
CN1739507A Medicine composition for treating mixed infectious disease The medicine composition for treating mixed infectious diseases contains tinidazole, bifonazole and chlorhexidine as main medicinal components and has the weight ratio among tinidazole, bifonazole and chlorhexidine of 1-10 to 1-10 to 1-10. It may be used to treat mixed infectious diseases effectively, especially mixed infectious vaginitis, liver abscess and other histozoic amebiasis, and acute and chronic amebosis.
CN103655223A Preparation with effects of preventing and treating acnes and application thereof The invention provides an azelaic acid oligopeptide preparation with effects of efficiently preventing and treating acnes and an application thereof in medical cosmetic. The preparation is synthesized from azelaic acid and oligopeptide under the effect of a catalyst. The azelaic acid oligopeptide synthesized by the invention has the characteristics of being good in water solubility, and significant in effect of preventing and treating acnes, low in side effect and the like. The cosmetic containing azelaic acid oligopeptide prepared by the preparation can be the dosage forms such as stoste, water aqua, facial mask, cream dew, liquid makeup, hair gel, essence and the like. The cosmetic is compounded by the azelaic acid oligopeptide and matrix. A lot of clinical tests prove that the medical cosmetic disclosed by the invention has the characteristics of being good in prevention and treatment of the acnes on the skin of a human body, good in nutrient, small in side effect and the like.
CN101332180A Melbex eye drops and preparation method thereof The present invention discloses an eye drop which contains 0.01 percent to 5 percent g/ml mycophenolic acid or a derivant of the mycophenolic acid as active component. The derivant of the mycophenolic acid comprises the medical acceptable salt or ester of the mycophenolic acid, such as mycophenolate sodium, mycophenolate mofetil. The eye drop can be combined with various kinds of components at will according to the clinical requirement to be made into different preparation forms, such as water soluble eye drop, oil soluble eye drop, emulsion type eye drop, suspension type eye drop and ointment, etc. The eye drop of the present invention is medicated in eyes directly to achieve the effect of anti-rejection and develops a new pathway for the mycophenolic acid and the derivant of the mycophenolic acid to be medicated in the eyes for remedying diseases. The experiment shows that the eye drop of the present invention has the characteristics of high comfort, no stimulation, being easy for absorbing, is safe for medicating in the eyes and has obvious anti-rejection effect.
US20100004323 Promoter construct A polynucleotide comprising a β subunit cGMP-phosphodiesterase promoter operably linked to one or more enhancer elements.
CN101906069A (S)-2-substituted-(3'-acetyl-2'-pyridone-1'-yl) acetic acid as well as preparation method and application thereof The invention discloses (S)-2-substituted-(3'-acetyl-2'-pyridone-1'-yl) acetic acid as well as a preparation method and application thereof. The preparation method thereof comprises the following steps of preparing N-acetoacetyl-L-amino acid methyl ester by condensing L-amino acid methyl ester and dicthenone; preparing N-[2-(5,5-dimethyl-1,3 dioxane-diyl-)vinyl]-N-acetoacetyl-L-amino acid methyl ester through reaction between N-acetoacetyl-L-amino acid methyl ester and 2-glyoxyl-5,5-dimethyl-1,3-dioxane; preparing (S)-2-substituted-(3'-acetyl-2'-pyridone-1'-yl) methyl acetate by the N-(2-(5,5-dimethyl-1,3 dioxane-diyl-)vinyl)-N-acetoacetyl-L-amino acid methyl ester; obtaining the (S)-2-substituted-(3'-acetyl-2'-pyridone-1'-yl) acetic acid by saponifying the (S)-2-substituted-(3'-acetyl-2'-pyridone-1'-yl) methyl acetate. A high-iron animal model is adopted to evaluate the detoxification activity when iron poisoning occurs in a compound body. An experimental result shows that the compound has excellent iron expulsion action and can be clinically used as antidote in the process of iron poisoning.
EP2479183A2 Polymorphs of sarsasapogenin The invention provides sarsasapogenin in novel amorphous, crystalline, solvated and hydrated forms, and the use thereof in manufacturing pharmaceutical or edible grade sarsasapogenin and its derivatives
WO2012011128A1 Preparation of prostaglandin derivatives A process for preparing the prostaglandin derivatives is provided, wherein the benzoyl and p-nitrobenzoyl groups are used as the hydroxyl protective groups. A pharmaceutical composition comprising the prostaglandin derivatives is also provided.
US20100099766 Topical NSAID compositions having sensate component Topical analgesic compositions comprising a topically administrable NSAID, a sensate agent and optionally a self-warming system, when administered to a patient in need thereof, provide significant improvements in the rate and extent of skin absorption, as well as impart a sensation of rapid and complete relief from pain.
WO2010128050A3 Dihydroorotate - dehydrogenasee inhibitors as virostatic compounds The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, for the use as a medicament.
WO2013049263A1 Substituted bicyclic heteroaryl compounds Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
CN103006608A Drug composition containing gefitinib The invention relates to a drug composition containing gefitinib, in particular to a tablet comprising the gefitinib. The tablet containing the gefitinib is made of the gefitinib with the particle size distribution as follows: D(0.1) is equal to 2-6mm, D(0.5) is equal to 11-20mm, and D(0.9) is equal to 35-50mm. According to the drug composition, active ingredients can be released continuously and stably, and the drug composition has a good treatment effect on the local advanced lung cancer or metastatic non-small cell lung cancer subjected to the chemotherapy in the past.
WO2006126505A1 Stat function inhibitor and application thereof When the expression of an EZI gene is inhibited using synthetic oligo-siRNA which targets the EZI gene or siRNA which has been expressed using a vector, the nuclear translocation of STAT3 and the activation of the expression of a STAT3-dependent gene are suppressed. A nucleic acid having a modification in an APRE sequence to which EZI protein and STAT3 protein can bind in the α2-macroglobulin promoter region inhibits the nuclear translocation/subcellular localization of STAT protein by EZI protein and also inhibits the activation of the expression of an STAT3-dependent gene. It is also found that a synthetic peptide having a cell membrane penetration signal bound to an STAT3-binding peptide on EZI protein inhibits the nuclear translocation/subcellular localization of STAT by EZI protein and the activation of the expression of an STAT-dependent gene and also inhibits the growth of cancer cells.
EP1307455B1 Inhibitors of alpha-l beta-2 mediated cell adhesion The present invention relates to a compound of formula: (I), or a pharmaceutically acceptable salt thereof.
CN101088505B Nanometer breviscapine polymer particle preparation and its preparation process The present invention relates to medicine, and is especially one kind of breviscapine-nanometer polymer preparation and its preparation process. The breviscapine-nanometer polymer preparation is prepared with breviscapine and nanometer polymer as carrier material in the weight ratio of 1 to 5-20. The breviscapine-nanometer polymer preparation has simple preparation process, and is applied clinically in treating cardiac and cerebral vascular diseases, such as cerebral thrombosis, cerebral infarction, coronary heart disease, etc.
WO2014076616A3 Formulations of 5-azacytidine The present invention relates to lyophilized formulations comprising Crystalline 5-azacytidine and process for preparing lyophilized formulations comprising Crystalline 5-azacytidine.
CN101862298A Benproperine phosphate granular formulation The invention provides a benproperine phosphate granular formulation comprising benproperine phosphate, flavoring agent, excipient, adhesive and solvent, wherein the weight ratio of benproperine phosphate to flavouring agent to excipient to adhesive is 2.64:4-6:170-190:190; and the flavouring agent can be one or two of Aspartame, Sodium cyclamate and citric acid. The benproperine phosphate granular formulation of the invention has the advantages of convenient carrying, accurate ration, favourable mouth feel and no degeneration after long term preservation and is very suitable for patients with dysphagia or children and elderly patients.
US7582654 Antiarrhythmia agents, treating gastrointensinal disorder, gastroesophageal reflux, chronic obstructive pulmonary disease, diabetes;N-cotnaining heterocyclic compound with carbamate or amide groups and indazole ring Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.
CN102641288A Nutrition combination for anti experiment beagle transportation stress The invention provides a nutrition combination for anti experiment beagle transportation stress, which is characterized by being composed of the following nutrients by weight: 8%-12% of vitamin B1, 5%-15% of vitamin B1, 18%-22% of vitamin C, 1%-3% of adenosine triphosphate (ATP), 4%-8% of edible sodium bicarbonate, 3%-5% of sodium chloride, 5%-9% of L-lysine hydrochloride, 3%-10% of inosine and 30%-40% of glucose. The nutrition combination has the advantages of being convenient to use, low in cost and capable of obviously reducing experiment beagle transportation stress symptom occurrence rate, quarantine observation time required by the experiment beagle to recover to the normal health condition and morbidity of the experiment beagle caused by transportation stress. The nutrition combination indicates that the nutrition combination is remarkable in anti experiment beagle transportation stress effect, and is capable of improving animal experiment speed and reducing animal experiment cost.
CN103054807A Curcumin micro-powder composition for intramuscular or hypodermic injection as well as preparation method and application thereof The invention discloses curcumin particles for injection, solvent specially used for the curcumin particles, and a preparation method and the application of the curcumin particles. The curcumin exists in a solid form, thus the curcumin is more easily stored and transported. Before clinical use, the curcumin micropowder for injection is dispersed in the special solvent; and the curcumin micropowder is dosed by intramuscular or hypodermic injection, so that the aim of treating diseases can be achieved.
US20080176813 Carbocyclic nucleosides and process for obtaining such The present invention provides a six membered, at least partially unsaturated, carbocyclic nucleoside compound, including the (−) enantiomer, the (+) enantiomer, and pharmaceutically acceptable salts and esters thereof. The compounds are represented by formula (I), wherein Z represents one double bond in the six membered carbocylic ring, B is a heterocyclic ring, such as a pyrimidine or purine base, X is an azido, F or OR2, R1 and R2 are the same or different and represent the same or different protecting groups, hydrogen, alkyl, alkenyl, acyl or phosphate moieties, and wherein the alkyl moiety is a saturated, optionally unsubstituted hydrocarbon having from 1 to 20 carbon atoms, the alkenyl moiety is an unsaturated congener of the alkyl group, and the acyl moiety is analkanoyl or aroyl moiety.
CN103124735A 4-alkylresorcinol derivative and external preparation for skin containing same Provided is a compound having a good skin lightening effect and excellent safety and stability, and an external agent for skin to which this compound is added. The compound is a 4-alkylresorcinol derivative represented by general formula (1) or a salt thereof. In the formula, R1 is a branched or cyclic C3-7 alkyl group or a linear C2-5 alkyl group, R2 and R3 are each independently a hydrogen atom or group represented by -P(O)(OR4)(OR5) and at least one of R2 and R3 is a group represented by -P(O)(OR4)(OR5), and R4 and R5 are each independently a hydrogen atom or linear or branched C2-5 alkyl group.
US20110064780 Polymeric pheromone formulation and method of use to calm stress-related behavior in mammals over an extended period of time The present invention is directed to a polymeric formulation for controlling animal behavior comprising a low melting point polymer or copolymer, an unsaturated long chain fatty alcohol, and an animal-appeasing pheromone to produce a solid slow release generator of the pheromone. The system is useful for making animal collars and the like.
US20120040978 Heterocyclic Fused Cinnoline M1 Receptor Positive Allosteric Modulators The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
US20100087470 Buprenorphine-Wafer for Drug Substitution Therapy The present invention relates to oral pharmaceutical dosage forms comprising buprenorphine with the dosage form releasing buprenorphine instantly upon oral, preferably sublingual, application of the dosage form. The present invention also relates to the use of such dosage forms for treating pain in a human or animal or for drug substitution therapy in drug-dependent human subjects.
US20080069840 Immunotherapy ; antigen codes Dna vaccine; antitumor agents An immunotherapeutic strategy is disclosed that combines antigen-encoding DNA vaccine compositions combined with siRNA directed to pro-apoptotic genes, primarily Bak and Bax, the products of which are known to lead to apoptotic death. Gene gun delivery (particle bombardment) of siRNA specific for Bak and/or Bax to antigen-expressing DCs prolongs the lives of such DCs and lead to enhanced generation of antigen-specific CD8+ T cell-mediated immune responses in vivo. Similarly, antigen-loaded DC's transfected with siRNA targeting Bak and/or Bax serve as improved immunogens and tumor immunotherapeutic agents.
WO2011155797A2 Hemioxalate salt of crystalline o-desmethylvenlafaxine, preparation method thereof, and pharmaceutical composition thereof The present invention relates to hemioxalate of crystalline O-desmethylvenlafaxine which maximizes solubility and has physicochemical properties of a solid material which is pharmaceutically preferable due to its non-hygroscopicity, to a preparation method of the hemioxalate, and to a pharmaceutical composition of the hemioxalate. The hemioxalate of crystalline O-desmethylvenlafaxine according to the present invention can: increase bioavailability of drugs due to its high solubility; allow various formulations to be very easily designed without composition size limitations; and administer high doses of drugs regardless of the dose-limiting volume of an animal. Thus, the hemioxalate of crystalline O-desmethylvenlafaxine facilitates the confirmation of expressible toxicity, and is suitable for distribution of raw materials and production of medicines because of low hygroscopicity.
CN103304445A Cation polyglycerol ester lipid and synthetic method and application thereof The invention belongs to the technical field of biology, and particularly relates to a brand-new cation lipid, namely a cation polyglycerol ester lipid, and a synthetic method and application thereof. The cation polyglycerol ester lipid is synthesized by coupling polyglycerol ester lipid and a nitrogen-containing micromolecular compound, wherein each molecule contains 1-8 or more nitrogen-containing groups. The cation polyglycerol ester lipid has the characteristics that a cation liposome with a particle diameter between 8 nanometers and 200 nanometers can be obtained by dispersing the cation polyglycerol ester lipid in water. The cation liposome can envelop a large quantity of nucleic acid drug molecules and realize the functions of nucleic acid drug molecules by transmitting the large quantity of nucleic acid drug molecules into cells on the cellular level, is very low in cytotoxicity and can realize an inhibiting effect on tumors by transmitting the large quantity of nucleic acid drug molecules to the tumor positions of tumor-bearing mice in a targeted way for enrichment on the animal level. The cation polyglycerol ester lipid disclosed by the invention has a wide application prospect as the vector of the nucleic acid drug molecules.
CA2858565A1 Methods of identifying and using mdm2 inhibitors Methods of treating subjects with cancer and screening for MDM2 inhibitors that may be effective cancer therapeutics are provided herein. The cancers that may be treated using SV1DM2 inhibitors using the methods described herein include those that are or may become resistant to treatment with tyrosine kinase inhibitors. Methods of treating subjects with cancers that have, or develop in response to treatment with tyrosine kinase inhibitors, elevated levels of MDM2, Mcl- 1 or PP5 or decreased levels of Huwel or CAS using MDM2 inhibitors are provided herein. The MDM2 inhibitors may be effective at treating these cancers alone or in combination with a tyrosine kinase inhibitor regardless of p53 states (mutant or wild-type) of the cancer.
WO2013039851A1 Optical agents for imaging and visualization of matrix metalloproteinase enzymes The invention relates generally to optical agents for biomedical applications including imaging, visualization, phototherapy and diagnostic monitoring of cells and tissue expressing MMPs and/or tissues associated with the expression of MMPs. In some embodiments, for example, optical agents of the present invention selectively bind to, or otherwise preferentially associate with, a target tissue expressing one or more MMPs, and function to couple electromagnetic radiation into and/or out of the target tissue, for example via optical absorption, fluorescence, scattering and/or optoacoustic processes.
EP2724707A2 Hair care products with anti-dandruff ingredients and a cationic keratin hydrolysate Cosmetic composition comprises, in a cosmetic carrier, (a) at least one anti-dandruff active substance that is present in an amount of 0.01-10 wt.% and comprises zinc pyrithione, climbazole, octopirox, ketoconazole, selenium disulfide, selenium-containing vegetable oils and selenium-containing plant extracts, and (b) at least one cationic keratin hydrolyzate present in an amount of 0.1-10 wt.%. An independent claim is included for treating keratinic fibers, comprising applying the cosmetic composition onto the keratinic fibers, and rinsing the cosmetic composition from the keratinic fibers after a contact time of a few seconds to 45 minutes.
WO2011082010A1 Tetrahydrotriazolopyridine compounds as selective mglu5 receptor potentiators useful for the treatment of schizophrenia The present invention provides certain tetrahydrotriazolopyridine derivatives, pharmaceutical compositions thereof, methods of using the same and processes for preparing the same. Formula (I) wherein R1 is hydrogen, fluoro, chloro, or methyl; and R2 is C4 - CS branched alkyl.
CN101612110B Triacetyluridine slow-release preparation and preparation method thereof The invention discloses a triacetyluridine slow-release preparation, which comprises (a) triacetyluridine, (b) a hydrophilic high polymer material, and (c) a pharmaceutically acceptable carrier, wherein the hydrophilic high polymer material is selected from one or more of hydroxypropyl methylcellulose (HPMC), hydroxy propyl cellulose (HPC) and sodium carboxymethylcellulose (CMCNa); the weight ratio of the triacetyluridine to the hydrophilic high polymer material is 1:0.3-2; and the sum of weight of (a), (b) and (c) in the low-release preparation accounts for 80 to 100 percent of the total weight of the preparation. The invention also discloses a preparation method for the preparation. The triacetyluridine slow-release preparation disclosed by the invention has high bioavailability, prolongs the action time in unit dosage to 8 to 12 hours, and obviously reduces fluctuation of plasma concentration.
US7531499 Spermine to facilitate absorption of cilostazol, rebamipide, cyclosporin and nifedipine The present invention provides a medicinal composition comprising (1) a pharmacologically active substance, (2) a drug absorbefacient and (3) a taurine compound or a polyamine. A taurine compound has an effect of suppressing or preventing damage of the intestinal mucous membrane, and therefore adding the taurine compound to a medicinal composition containing a pharmacologically active substance and a drug absorbefacient makes it possible to suppress or prevent damage of the intestinal mucosa. A polyamine improves the absorbability of pharmacologically active substances, and therefore adding the polyamine to a medicinal composition containing a pharmacologically active substance and a drug absorbefacient makes it possible to decrease the dose of the drug absorbefacient, thereby suppressing or preventing damage of the intestinal mucosa.
US7232835 3,6-Disubstituted azabicyclo derivatives as muscarinic receptor antagonists This invention relates to derivatives of 3,6-disubstituted azabicyclo compounds. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.
US20080255074 Citalopram, S-citalopram, clomipramine, fluoxetine, fluvoxamine, paroxetine, sertraline; glucocorticoid receptor antagonist (11 beta ,17 beta )-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one) The invention provides for a combination comprising an amount of an SSRI, or a pharmaceutically acceptable salt or solvate thereof, and an amount of a GR antagonist, or a pharmaceutically acceptable salt or solvate thereof, optionally in association with one or more pharmaceutically acceptable carriers for use as therapy for depression and related disorders.
WO2005005390A1 Novel enzyme inhibitor A novel naphthalene derivative that is useful as a medicinal drug, especially C17-20 lyase inhibitor. The C17-20 lyase is one of enzymes for sex hormone biosynthesis which are present in the testicle, ovary and adrenal cortex. The C17-20 lyase produces dehydroepiandrosterone and androstenedione from 17-hydroxyprognenolone and 17-hydroxyprogesterone as substrates. The biosynthesis by this enzyme is used only in biosynthesis of sex hormone, so that the novel naphthalene derivative capable of inhibiting the enzyme presents a novel endocrinotherapeutic agent capable of inhibiting the biosynthesis of sex hormone and is useful as a therapeutic or preventive drug.
EP2470171A1 Antimicrobial amino-salicylic acid derivatives Disclosed is a novel method for achieving an antimicrobial, preservative and/or microorganism adhesion inhibiting effect, for the protection within an article and/or material or on the surface of an article and/or material. The novel method comprises application of a salicylic compound of the formula (I) wherein one of A and A is a residue of the formula (I'): -NH-CO-R1 while the other is hydrogen; R1 is C1-C22alkyl, C3-C12cycloalkyl, C3-C12cycloalkyl interrupted by O and/or NR5, C4-C12aryl, C5-C18arylalkyl; R2 is OR3 or NHR4; R3 and R4 are selected from H, C1-C22alkyl, C3-C12cycloalkyl, C3-C12cycloalkyl interrupted by O and/or NR5, C4-C12aryl, C5-C18arylalkyl; R5 is H or C1-C8alkyl; wherein each aryl moiety is unsubstituted or substituted by C1-C4alkyl, C1-C4alkoxy, C1-C4acyl, C1-C4acyloxy, C1-C4acylamino, CF3, OH, amino, halogen; or an adduct or salt thereof; to said article and/or material.
CN102836133A Sodium aescinate freeze-dried powder injection and preparation method thereof The invention discloses a sodium aescinate freeze-dried powder injection which has single preparation component and high stability and is free from irritation and a preparation method thereof. The freeze-dried powder injection comprises sodium aescinate serving as a major agent, tert-butyl alcohol serving as a freeze-drying protective additive and water for injection in the mass ratio of 1:(50-300):100. The preparation method comprises the following steps of: dissolving sodium aescinate into tert-butyl alcohol; stirring for dissolving; adding water for injection, mixing and stirring to obtain a clear and bright solution; and performing adsorption decarburization, filtration sterilization and split charging freeze drying to obtain a sodium aescinate freeze-dried powder injection. The sodium aescinate freeze-dried powder injection prepared with the method disclosed by the invention can be produced efficiently on an industrial scale by adopting the conventional process equipment; and moreover, a process is simple, a tert-butyl alcohol-water cosolvent can be recycled, preparation cost is saved, and discharge of waste is reduced.
CN102641241A Sarafloxacin hydrochloride suspension emulsion and preparation method thereof The invention relates to a preparation method of a sarafloxacin hydrochloride suspension emulsion, wherein the sarafloxacin hydrochloride suspension emulsion is prepared from 10-30% of sarafloxacin hydrochloride, 5-15% of emulsifying agent, 20-30% of oil phase, 0.02-5% of auxiliary stabilizer and the balance of water. The method has the following advantages: the drug is a mixed system with a water phase, an oil phase and an solid phase, therefore, the suspension emulsion has excellent properties of a suspension and an emulsion; the dosage of an intramuscular injection drug is reduced; intracorporal stimulation to livestocks is low; and if being applied, the drug is dispersed in micronized drug active ingredients in the water phase and the oil phase and slowly released in a human body to achieve the effects of targeting and slow release and long acting. In addition, the drug-loading rate of the suspension emulsion is great and the properties of the suspension emulsion are stable; and after being stood and transported, the suspension emulsion has less possibility of being layered and settled; besides, the suspension emulsion is good in flowability and convenient for intramuscular injection; and therefore, a new way for the application of the sarafloxacin hydrochloride in veterinary clinic is opened up.
WO2011049908A2 Bismacrokyclic compounds as hepatitis c virus inhibitors The present invention discloses compounds of formula (Ia) or (Ib) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
US20110123486 Methods of treating multiple myeloma and resistant cancers Erastin analogs are useful in treating various cancers, particularly multiple myeloma. Erastin analogs are also useful in treating cancers that are resistant to other anticancer agents.
EP1965779A1 Compositions and methods of sensitizing methicillin resistantstaphylococcus aureus to oxacillin Contemplated methods and compositions further increase susceptibility of sensitized MRSA against various antibiotic drugs. Most preferably, the MRSA is already sensitized with a galloylated catechin (e.g., ECG), and further sensitization is achieved by exposure to a non-galloylated catechin (e.g., EC), and most preferably the corresponding non-galloylated catechin.
WO2009148599A1 Pyrrole compunds that modulate hsp90 activity The present invention relates to substituted pyrrole compounds and compositions comprising substituted pyrrole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted pyrrole compound of the invention, or a pharmaceutical composition comprising such a compound.
CN103417987A Application of miR-148 to proliferation of pancreatic beta cells The invention relates to the field of biology and medical drugs, and discloses the function of miR-148 on proliferation and apoptosis of pancreatic beta cells, which provides a new target spot for diabetes treatment as well as preparation or screening of drugs for curing 2-type diabetes. According to the invention, miR-148 can be applied to the preparation or screening of drugs for controlling pancreatic beta cells, and preparation or screening of drugs for controlling apoptosis of pancreatic beta cells, or preparation or screening of drugs for curing 2-type diabetes.
WO2010061282A1 Derivatives of [(3-hydroxy-4 pyron-2-yl)methyl]-amine and use thereof as anti-neoplastic drugs The present invention relates to compounds having general formula (I), i.e. poly- alkyl -bis -maltolic molecules and in particular to derivates of [ (3 -hydroxy- 4 -pyron- 2 -yl) methyl] -amine and pharmaceutically acceptable salts thereof, and to the use thereof as anti -neoplastic drugs, in particular, for the preparation of a medicament for the treatment of neoplastic diseases.
EP1267828B1 Pharmaceutical preparations containing saccharose fatty acid esters for controlling the release of active ingredients The invention relates to novel oral pharmaceutical formulations having a variably adjustable release effect . Said formulations contain one or several sucrose fatty acid esters as exclusive release control agents, in addition to one or several active ingredients. The invention also relates to a method for the production of the formulations by fusion granulation or fusion pelletizing . The novel pharmaceutical formulations range from quick release to delayed release medicament forms.
US7122206 Spraying into nose; triamcinolone acetonide An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (D) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively high and such that it resists being cleared from the mucosal surfaces by the inherent mucocillary forces which are present in the nasal cavity, a method of use of the composition and a method for preparation of the composition, including in preferred form the use of anti-inflammatory steroid, for example, triamcinoline acetonide, and an odorless form of the composition.
WO2014059202A1 Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
WO2011066176A1 Process for preparing a polymorph of the choline salt of a pyrimidin-5-yl acetic acid derivative Provided is a process for preparing a choline salt of [4,6-bis(dimethylamino)-2-(4-{ [4- (trifluoromethyl)benzoyl] amino }benzyl)pyrimidin-5-yl] acetic acid. The process of the invention is useful for preparing the salt in purer forms of the salt. Also disclosed is a more pure form of the of choline salt of [4,6-bis(dimethylamino)-2-(4-{ [4- (trifluoromethyl)benzoyl] amino }benzyl)pyrimidin-5-yl] acetic acid.
US20120129949 Use of Anthracene Derivatives as Anti-Infectives The present invention relates to the use of the following anthracene derivatives as anti-infectives, preferably against multiply drug resistant pathogens: (2R,3S,10R)-2,3,5,10-tetrahydroxy-6-methoxy-3-methyl-1,2,3,4,4a,9a-hexahydro-9H,10H-anthracen-9-one (tetrahydroaltersolanol B), (1R,2R,3R,4aS,9aR,10R)-1,2,3,5,10-pentahydroxy-7-methoxy-2-methyl-1,2,3,4,4a,9a-hexahydro-9H,10H-anthracen-9-one (altersolanol K), (2R,3R,4R,4aS,9aS,10R)-2,3,4,8,10-pentahydroxy-6-methoxy-3-methyl-1,2,3,4,4a,9a-hexahydro-9H,10H-anthracen-9-one (altersolanol L), 8-(1,7-dihydroxy-6-methyl-3-methoxy-9,10-dioxo-9H,10H-anthracen-2-yl)-(1S,2S,3R,4S)-1,2,3,4,5-pentahydroxy-7-methoxy-2-methyl-1,2,3,4-tetrahydro-9H,10H-anthracen-9,10-dione (atropisomers alterporriol G and H); as well as (2R,3S,4aS,9aS,10R)-2,3,5,8,10-pentahydroxy-6-methoxy-3-methyl-1,2,3,4,4a,9a-hexahydro-9H,10H-anthracen-9-one (8-hydroxytetrahydroaltersolanol B).
US6939563 Use of a polyol selected from polyoxyethylene glycol or ethylene glycol-propylene glycol copolymer, a non-fermented osmotic laxative as an anticarcinogenic agent for treating colon or rectum cancer Use of a non-fermented osmotic laxative as an active agent for preparation of a medicinal product for treating and/or preventing colon and/or rectum cancers. A method of treating or preventing colon or rectum cancer comprising administering to a mammal a therapeutically effective amount of a non-fermented osmotic laxative.
CN102670510A Tripterine nanostructure lipid carrier modified by lentiviral vector and appliance for preparing and treating prostatic cancer, lung cancer and breast cancer drug The invention discloses a tripterine nanostructure lipid carrier modified by lentiviral vector and preparation method and application thereof, wherein teh tripterine nanostructure lipid carrier modified by the lentiviral vector consists of tripterine and a lipid carrier, various components comprise 1 part by weight of tripterine, 0.5 to 10 parts by weight of lentiviral vector, 5 to 100 parts by weight of lipid blends, 0.5 to 20 parts by weight of emulsifier and 5 to 100 parts by weight of stabilizer. The tripterine nanostructure lipid carrier modified by the lentiviral vector can increase nanoparticles encapsulating rate to 78-90%. The tripterine nanostructure lipid carrier modified by the lentiviral vector uses oral administration, thereby promoting absorbing of the tripterine in a body,improving bioavailability, reducing administration dosage, reducing accumulation of the tripterine in the body at last, reducing toxic reaction by combining sustained release of a nanostructure lipidcarrier, and improving clinical therapeutic effect of the tripterine at last.
US20090048261 Pharmaceutical Composition for Treatment of Ocular Hypertension The present invention is related to the pharmaceutical industry in general and in particular with the pharmaceutical industry of production of ophthalmic compositions. More specifically, the present invention relates to the pharmaceutical industry of production of ophthalmologic compositions for the treating of ocular hypertension. The advantage of the present invention against the present state of the technique is the fulfilling of a synergic effect of its components for the decreasing of ocular hypertension with no antagonistic effect between its components. The present invention consists of a pharmaceutical composition for the treatment of ocular hypertension characterized by comprising a pharmacologically effective amount of dorzolamide, with a pharmacologically effective amount of timolol and a pharmacologically effective amount of brimonidine.
US20100092477 Methods and compositions for treating prostate cancer A polypeptide comprising an androgen binding region, the androgen binding region capable of binding to an androgen at a sufficient affinity or avidity such that upon administration of the polypeptide to a mammalian subject the level of biologically available androgen is decreased. Specifically disclosed is an AR IgG1 Fc fusion protein, comprising the androgen binding domain of human androgen receptor and the Fc region of IgG. This fusion protein is used in the treatment of prostate cancer and testosterone flare.
US20100215619 Hla peptide therapy The invention provides polypeptides derived from a major histocompatibility complex (MHC) class I human leukocyte antigen (HLA), such as HLA-A2, and derivatives or analogues thereof. The polypeptides, derivatives and analogues can be used to treat or prevent allosensitisation, such as the treatment or prevention of allograft rejection.
WO2009140863A1 Compositions comprising quinazoline derivatives, preparation methods and uses thereof Pharmaceutical compositions, which comprise pharmaceutically acceptable salts of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazoline-6-yl}-acrylamide and optional, medically applicable carriers or diluents, are provided. The said compositions also comprise stabilizers which function as dispersing and/or protecting the active components. Pharmaceutical preparations containing the compositions, methods of preparing the compositions and preparations, and their uses in the treatment of disorders characterized by aberrant erbB family PTKs activity in mammals, are also provided.
CN102793683A Slow release composition containing levomilnacipran and preparation method of composition The invention relates to a slow release composition containing levomilnacipran and a preparation method of the composition. The composition contains the following component in parts by weight: 10-70 parts of levomilnacipran or pharmaceutically acceptable salts thereof as an active ingredient and is characterized in that the composition also comprises the following components in parts by weight: 5-30 parts of high-viscosity hydroxypropyl methylcellulose as a hydrophilic gel slow release framework material and 3.5-7.5 parts of acrylic resin as a pH regulator. During preparation, the levomilnacipran, hydroxypropyl methylcellulose and acrylic resin are mixed fully and uniformly. The composition can achieve consistency of release behaviors in artificial gastric fluid and artificial intestinal fluid and sustained release effect can be kept for 12 hours; and the composition is low in preparation losses, high in efficiency and good in stability, simple to operate and easy to popularize.
EP1248618B1 Polymorphic, amorphous and hydrated forms of 5-chloro-3-(4-methanesulfonylphenyl)-6'-methyl- 2,3']bipyridinyl Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase -2 (COX-2) inhibitor.
US7109189 Mitochondrially targeted antioxidants The invention provides mitochondrially targeted antioxidant compounds comprising a lipophilic cation moiety covalently coupled to a glutathione peroxidase mimetic. These compounds can be used to treat patients who would benefit from the reduction of oxidative stress.
DE102010026471A1 Use of a sulfur preparation for producing a medicament for the treatment of asthmatic diseases, where the sulfur variant is aqua brimstone Use of a sulfur preparation for the treatment of asthmatic diseases, where the sulfur variant is aqua brimstone, is claimed. - ACTIVITY : Antiasthmatic; Virucide. - MECHANISM OF ACTION : None given.
US20120329828 Cocaine Analogs and Methods of Preparation and Uses Thereof The invention provides novel cocaine analogs. The invention also provides a method of preparing cocaine analogs with control over the substituents installed at the C-1, C-2, C-3, C-4 and N-8 positions of the tropane bicyclic scaffold. The invention further provides methods of providing anesthesia, blocking reuptake of a monoamine neurotransmitter, and treating depression, by administering to a subject in need of such treatment a pharmaceutical composition comprising a compound of the invention.
WO2008040153A1 Application of a coumarin compound in preparation of medicament for inducing nerve stem cell orienting differentiation Use of a coumarin compound in preparation of medicament for inducing nerve stem cell orienting differentiation. The typical coumarin compound is aesculetin, 7-hydroxycoumarin, megeresin, daphnoretin, aesculetin glucoside and scopoletin. The test has proved that it has significant induced nerve stem cell orienting differentiation function and can be used to treat demyelinating diseases and spinal cord injury. The prepared medicament comprises the said coumarin compounds as active component, with pharmaceutically acceptable carriers, while the content of the active component is 0.1~99.5%(wt), and the formulation thereof is tablet, powder, granule, injection etc.
CN1562036A Nutrition supplement agent A nutrients supplementing medicine contains folic acid, VD, calcium carbonate and auxiliaries.
US7153997 N-hydroxyphenoxyphenyl derivatives of glycine or valine, e.g., N-[3,5-Dichloro-4-(4-hydroxy-3-isopropyl-5-methylphenoxy)benzoyl]glycine; treating metabolic disorders or diseases dependent upon the expression of a T3 regulated gene This invention relates to novel compounds, which are thyroid receptor ligands, and to methods of preparing such compounds. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described herein is administered in a therapeutically effective amount.
US7098213 three-ring saturated N-heterocyclic compounds in combination with one or more antiviral or other agents; in immunotherapy Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ═O, ═NOR10, ═N—NR11R12 or ═CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9–R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, graft v. host disease, inflammatory diseases, atopic dermatitis, asthma, allergies or multiple sclerosis, as well as pharmaceutical compositions and combinations with antiviral or anti-inflammatory agents.
WO2014085684A1 Gastric health supplement and methods thereof The invention provides novel compositions that can be used as a supplement (e.g. feed supplement) to animals such as, horses. In certain embodiments, the composition comprises an effective amount of a preparation obtained from sea buckthorn and an effective amount of an amino acid. In other embodiments, the composition includes specific combinations of components selected from the group of a preparation obtained from sea buckthorn, glutamine, aloe vera extract, pectin, and lecithin. The invention also provides methods and uses of the composition for alleviating, treating or preventing an ulcer-related condition in a subject identified in need thereof.
US8268343 Non-hormonal vaginal contraceptive The present invention relates to a non-hormonal, biocompatible, and biodegradable intravaginal device for the delivery of spermiostatic, spermicidal and anti-infectious agents. The present invention also relates to methods of contraception using such a device, as well as the prevention and treatment of sexually transmitted diseases and vaginal infections through the application of the device.
WO2007090733A1 Nitrooxy derivatives suitable as alpha2 adrenergic receptor agonists Alpha 2 adrenergic agonist nitrooxyderivatives of formula (I): A-(X0-ONO2)s(I) and enantiomers and diastereoisomers and pharmaceutically acceptable salts thereof, wherein: s is an integer equal to 1, 2 or 3; wherein A is a precursor of an alpha 2 adrenergic receptor agonists having wider pharmacological activity and enhanced tolerability. They can be employed for treating cardiovascular disease, in particular systemic hypertension, renal and chronic liver diseases, inflammatory processes and metabolic syndromes.
CN103561738A Ropinirole-containing adhesive patch and packaging therefor A ropinirole-containing adhesive patch provided with an adhesive layer and a carrier layer, the adhesive layer containing ropinirole and/or a pharmaceutically acceptable salt thereof, wherein the amount of ropinirole and/or pharmaceutically acceptable salt thereof contained in the adhesive layer, calculated in terms of ropinirole educt, is 5-13.2 mass% relative to the total mass of the adhesive layer.
CN102001996A Compound for inhibiting growth of tubercle bacillus and preparation method thereof The invention relates to a compound for inhibiting the growth of tubercle bacillus and a preparation method thereof, belonging to the field of chemical synthesis. The invention provides 1-ethyl-4-hydroxy-2-oxygen-N'-trideformoxyl-1,2-dihydroquinoline-3-formylhydrazine with the structure of general formula (I) or pharmaceutically acceptable nontoxic salt thereof aiming at more and more serious epidemic situation of tuberculosis and the occurrence of multiple-drug resistant tuberculosis. In vitro tubercle bacillus inhibition tests verify that the compound of the invention can effectively inhibit the growth of tubercle bacillus, the MIC (Minimal Inhibitory Concentration) range is 0.4-2 mu g/ml, and moreover, the compound also has obvious inhibition effects on the growth of multiple-drug resistant tubercle bacillus in clinic.
US20110082178 Methods of treating autoimmune and inflammatory diseases and disorders Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed. Particular compounds are of formula I:
CA2845673A1 Pharmaceutical nanoparticle compositions This invention relates to the use of nanoparticles of glucocorticoid antagonists for the treatment of ocular and non-ocular conditions, compositions containing them and methods for the preparation thereof.
CA2302838C Modulation of the sphingosine kinase signalling pathway The present invention relates to a sphingosine kinase signalling pathway via which cellular activities such as adhesion molecule expression are achieved. By regulating the expression and activity of individual components of this pathway, these cellular activities can be modulated. The present invention also contemplates a rapid, high volume assay for detecting agents exhibiting sphingosine kinase and agents that can act as agonists and antagonists of these sphingosine kinase activity.
WO2010121324A1 A novel formulation of metaxalone The present invention relates to methods for producing particles of metaxalone using dry milling processes as well as compositions comprising metaxalone, medicaments produced using metaxalone in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of metaxalone administered by way of said medicaments.
EP1213975B1 Method for extracting compounds of furan lipids and polyhydroxylated fatty alcohols of avocado The invention concerns a method for selectively extracting furan lipids and polyhydroxylated fatty alcohols of avocado, characterised in that it comprises steps which consist in: preparing an unsaponifiable matter of avocado; then in subjecting the unsaponifiable matter of avocado to a step of molecular distillation using adjusted temperature and pressure means to obtain either a distillate comprising mainly furan lipids and polyhydroxylated fatty alcohols of avocado. Said method enables in particular to extract selectively furan lipids of avocado having a furan lipid content of more than 80 wt. %, even close to 98 %.
CN102675205A Pyrazol oxime ether compound and preparation method and application thereof in anticancer therapy The invention discloses a pyrazol oxime ether compound and a preparation method and application thereof in anticancer therapy. The invention has the advantage that: the pyrazol oxime ether compound has a function of inhibiting human cervical cancer Hela cell proliferation, so that the pyrazol oxime ether compound can be used as a potential anti-tumor drug.
CN1939302A Siromosi medicinal composition and its making method A composite medicine in the form of tablet or capsule is prepared from sirolimus, the carrier chosen from povidone K30, poloxamer 188 and vitamin-E polyethanediol succinate, and auxiliary. Its preparing process is also disclosed.
CA2321819C Xylitol compositions for treating upper respiratory conditions Xylitol/xylose compositions and their methods of use for the treatment or prevention of nasopharyngeal congestion, recurrent sinus infections, infection or inflammation associated with bacteria, or asthma triggered by upper respiratory inflammation by nasal administration of the xylitol/xylose compositions are disclosed.
CN1951373A Method for preparing nimodipine dispersible tablet with high dissolution The invention relates to a method for preparing soluble Dunimodi disperser. Wherein, it comprises that using the Dunimodi material and hydrophilic carrier, via fusion protrusion technique, to prepare their sosoloid; breaking the sosoloid, to be mixed with stuff, lubricant and surface activator into tablet. The invention has simple process while the product has high dissolve speed, the drug can be released as molecule, to improve its utilization.
CN103690954A Cardiovascular protection medicinal composition and use thereof The invention discloses a cardiovascular protection medicinal composition, which comprises 5 to 200 mole parts of an angiotensin-converting enzyme inhibitor and 100,000 to 600,000 mass parts of an antioxidant. The invention also discloses the use of the medicinal composition and a blood substitute. The cardiovascular protection medicinal composition can be used for effectively protecting the cardiovascular system and lowering the cardiovascular side effects of a hemoglobin-based oxygen carrier. The blood substitute has no cardiovascular side effects, and has a broad clinical application prospect, and the shortcomings of a conventional hemoglobin blood substitute are overcome.
WO2009092912A1 Method for the preparation of morphine compounds The present invention relates to a method for the preparation of morphine compounds comprising a low content of α,β-unsaturated compounds, which comprises the steps of: (i) bringing the crude morphine compound into contact with a base, at a pH of greater than 13, under conditions which make possible the Michael addition reaction on the α,β‑unsaturated compound(s) present; (ii) separating the morphine compound from the reaction mixture; and (iii) if appropriate, separating the addition product formed, from the morphine compound. It also relates to a composition comprising at least 99% by dry weight of morphine compound, or of a pharmaceutically acceptable salt thereof, and an α,β‑unsaturated compound in a content of less than 100 ppm.
US7176232 Fermentation product of marine actinomyces strains; antiproliferative agents; anticancer agents The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
US20070037836 Melanin concentrating hormone; obesity and related disorders, anxiety, or depression; trans-4-Bromo-N-{4-[(4-dimethylamino-quinazolin-2-ylamino)-methyl]-cyclohexylmethyl}-2-trifluoromethoxy-benzenesulfonamide The present invention relates to novel compounds of the formula (I) which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of obesity, obesity related disorders, anxiety, or depression.
CN101884791A Latrozole co-ground material, preparation method thereof and medicament composition having same The invention discloses a Latrozole co-ground material, a preparation method thereof and a medicament composition having the same. The Latrozole co-ground material comprises Latrozole and a hydrophilic material in a mass ratio of 1:0.5 to 1:20, wherein the hydrophilic material is one or more of polyethylene glycol, lactose, starch, starch derivatives, povidone and mannitol; and an average grain diameter of Latrozole grains is 1 to 100 mu m. In the medicament composition prepared from the Latrozole co-ground material, the dissolution rate of the Latrozole is obviously improved, and the medicament composition has a simple preparation method and is particularly suitable for industrial production.
WO2010094659A1 Amine or amino alcohols as glyt1 inhibitors The invention relates to the use of compounds of formula (I), wherein the substituents are described in the description and claims, for the preparation of medicaments for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease.
WO2011017319A1 Methods of treating disorders associated with protein polymerization The present invention relates to methods of treatment of clinical disorders associated with protein polymerization comprising administering, to a subject, an effective amount of carbamazepine, oxcarbazepine or another carbamazepine-like compound. It is based, at least in part, on the discovery that, in cells having a genetic defect in α1-antitrypsin, carbamazepine was able to decrease levels of the mutant protein. Furthermore, carbamazepine reduced the hepatic load of mutant α1 -antitrypsin and the toxic effect of that mutant protein accumulation, hepatic fibrosis, in vivo using a mouse model of the disease. As patients having this defect in α1 -antitrypsin exhibit toxic accumulations of the protein, treatment according to the invention may be used to ameliorate symptoms and signs of disease.
CA2781780A1 Novel antiviral compounds The present invention relates to compounds of formula (A) as defined herein having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical 5 compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the 10 administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
WO2014089416A1 Compositions comprising anti-cd38 antibodies and lenalidomide Disclosed herein are compositions and kits which comprise anti-CD38 antibodies and lenalidomide compounds. Also disclosed are methods for treating cancers, such as multiple myeloma, in subjects with the compositions and kits.
US7459458 Polymorph of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto Polymorph Form III of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide, and use thereof as a sedative-hypnotic, anxiolytic, anticonvulsant, and/or skeletal muscle relaxant agent. Related compositions and methods are also disclosed, particularly with regard to treatment of insomnia.
US20120070385 Methods for Treating Cognitive/Attention Deficit Disorders Using Tetrahydroindolone Analogues and Derivatives The present specification discloses tetrahydroindolone derivatives or analogues and methods for treating cognitive/attention deficit disorders using such tetrahydroindolone derivatives and analogues.
US20050154232 Nitrosation of the diphenylamine with an alkali metal nitrite in an acidic medium; the nitrosodiphenylamines increase the bioavailability of endothelial nitrogen monoxide; the diphenylamines are used as antioxidants and free radical scavengers; insulin resistance Compounds of formula (I) in which each of the phenyl rings represented is optionally substituted one or more times; n represents an integer selected from 0, 1, Z, 3, 4 and 5; W represents —CO— or —SO—2; Z represents H; alkyl; aryl; or arylalkyl R1 represents any monovalent organic group; and the pharmaceutically acceptable salts thereof, can be used in the treatment of pathologies that are characterized by an oxidative stress condition.
CN103356538A Application of Sarcaboside A in preparation of drug for treating ovarian cancer The invention discloses application of Sarcaboside A in preparation of a drug for treating ovarian cancer, which belongs to the technical field of new applications of drug. According to the invention, the in-vitro MTT (Methyl Thiazolyl Tetrazolium) antitumor activity evaluation discovers that Sarcaboside A also has an obvious inhibiting effect on the growth of human ovarian cancer cell strains HO-8910, HOC1 and OVAC. Thus, Sarcaboside A can be used for preparing an anti-ovarian cancer drug and has good development and application prospects. The application of Sarcaboside A in preparation of the drug for treating ovarian cancer is disclosed by the invention for the first time. The skeleton type is brand new and Sarcaboside A has unexpectedly strong inhibitory activity to the human ovarian cancer cell.
US20050090474 Methods and compositions for enhancing and inhibiting fertilization A method of contraception is provided. The method comprises providing to a subject an amount of a p38 activator and/or an ERK inhibitor capable of substantially reducing sperm motility. Also provided is a method of enhancing fertility comprising providing to a subject a therapeutically effective amount of a p38 inhibitor and/or an ERK activator, thereby enhancing fertility.
US20080206187 thermal ablation; polyethylene oxide-polypropylene oxide copolymer sensitizes neoplastic cells to hyperthermia A method for treating a neoplastic disorder in a subject includes administering to the neoplastic cells a neoplastic cell-sensitizing composition including a poly(ethylene oxide)-poly(propylene oxide) copolymer. The poly(ethylene oxide)-poly(propylene oxide) copolymer can sensitize the neoplastic cells to hyperthermia. Energy can be applied to the neoplastic cells to heat and ablate the cells.
US7253171 Antiinflammatory agents; immunology diseases; multiple sclerosis; antihistamines; antidiabetic agents; vision defects; antiarthritic agents; skin disorders; antitumor agents Novel antagonists of ∝4β1 integrin and/or ∝4β7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4.
CN103153344A Methods, compositions, and kits for the treatment of matrix mineralization disorders The present invention provides methods, compositions, and kits for the treatment of matrix mineralization disorders such as hypophosphatasia. In particular, the present invention provides polypeptides having a soluble alkaline phosphatase fused to an Fc domain of an immunoglobulin. Such polypeptides can be administered to patients, e.g., subcutaneously, to treat hypophosphatasia using enzyme replacement therapy. The invention also features nucleic acids encoding such polypeptides and the use of the nucleic acids for treating matrix mineralization disorders.
EP2291193A1 Preparation of intermediates useful in the syntheis of 2'-cyano-2'-deoxy-n4-palmitoyl-1-beta-d-arabinofuranosylcytosine The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2'; (ii) converting said compound of formula 682-2' into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2'-cyano-2'-deoxy-N4 -palmitoyl-1-β-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
CN103536593A Use of pyrroloquinoline quinone in preparing medicines for preventing and treating tumors The invention discloses use of pyrroloquinoline quinone in preparing medicines for preventing and treating tumors. Experiments prove that pyrroloquinoline quinone has relatively strong cytotoxicity to human lung cancer cells (A549) and mouse neuroblastoma cells (N2a) and is in a same order of magnitudes with positive control cis-platinum. The pyrroloquinoline quinone exists in diet of people and further exists in living bodies, is widely distributed in tissues and organs of human body, and exists in breast milk. Long-term use proves that pyrroloquinoline quinine is high in safety.
WO2004110492A3 Composition comprising triptans and nsaids A pharmaceutical composition comprising a 5HT1 receptor agonist or a pharmaceutically acceptable derivative thereof in combination with an NSAID or pharmaceutically acceptable derivative thereof wherein the 5HT1 receptor agonist and NSAID are located in discrete zones with respect to each other wherein each zone comprises the active ingredient and optionally a carrier. A preferred composition comprises sumatriptan succinate and naproxen sodium.
US7718627 Plasmid comprising nucleotide sequences coding immunoglobulin complementary determining regions specific to tumor antigen (5T4); for use in delivering product and/or nucleotide sequences of interest to tumor; drug delivery A vector comprising a nucleotide sequence of interest (“NOI”) encoding a product of interest (“POI”) is described. The NOI and/or the POI is capable of recognizing a tumor, such that in use the vector is capable of delivering the NOI and/or the POI to the tumor.
CN103007253A Pharmaceutical composition containing beta-galactosylation azo ene glycol and preparation method thereof The invention relates to the technical field of medical pharmaceutical engineering, relates to a pharmaceutical composition containing an NO donor and a preparation method thereof, in particular to a pharmaceutical composition containing beta-galactosylation azo ene glycol and a preparation method thereof. The pharmaceutical composition containing beta-galactosylation azo ene glycol provided by the invention comprises NO donor medicine containing beta-galactosylation azo ene glycol, sperm of xenopus laevis, montmorillonite and moisture-proofing agent; and the preparation method of the pharmaceutical composition comprises the following steps of: dissolving sperm of xenopus laevis in alcoholic solution, adding montmorllonite, fully stirring, filtering the montmorillonite, and drying; dissolving the NO donor medicine containing beta-galactosylation azo ene glycol in alcohol, then adding the montmorllonite, fully stirring, filtering the montmorillonite, volatilizing the alcohol and then adding the moisture-proofing agent, and mixing evenly, thus the pharmaceutical composition containing beta-galactosylation azo ene glycol is obtained. The pharmaceutical composition containing beta-galactosylation azo ene glycol provided by the invention is waterproof and antiacid, release time of the NO donor can be prolonged, and stable and controllable aims are achieved.
WO2012177678A2 Isotopologues of pomalidomide Provided herein are pomalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.
US20090069326 (R)-3-{3,5-Dichloro-4'-[4-(2-fluoro-ethyl)-piperazine-1-carbonyl]-biphenyl-4-ylmethyl}-1-(4,4-difluoro-cyclohexyl)-pyrrolidin-2-one, used for the treatment of diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome and cognitive disorders The present invention discloses novel compounds of Formula I: (I) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11β-HSD type 1 activity.
US7479563 Method of producing polymorphic crystals of donepezil hydrochloride The present invention provides a simple method of producing polymorphic crystal (III), which has high safety to environment and the bodies of operators; is gentle to environment; and can produce at low costs; and has a high refining effect. It is a method of producing polymorphic crystal (III) of donepezil hydrochloride (chemical name: 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine•monohydrochloride) represented by the following structural formula (formula (I)), which comprises dissolving donepezil (chemical name: 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine) in ethanol; and adding hydrochloric acid or hydrogen chloride thereto, followed by stirring.
US20090124598 Pharmaceutical use of substituted amides The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
US20090246183 eNOS mutations useful for gene therapy and therapeutic screening The present invention relates to new NOS variants or mutants which contain structural alterations in the site of Akt dependent phosphorylation. The altered NOS proteins or peptides, especially the human eNOS proteins or peptides, Akt proteins or polypeptides and their encoding nucleic acid molecules are useful as gene therapy agents for the treatment of diseases including post angioplasty restenosis, hypertension, atherosclerosis, heart failure, diabetes and diseases with defective angiogenesis. NOS proteins and peptides are also useful in methods of screening for agents which modulate NOS activity.
WO2009068955A2 Polymorphs of a c-met/hgfr inhibitor This invention relates to polymorphs of 2-[4-(3-Quinolin-6-ylmethyl-3H- [1,2,3]triazolo[4,5-b]pyrazin-5-yl)-pyrazol-1-yl]-ethanol that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to compositions including such salts and polymorphs, and to methods of using such compositions in the treatment of abnormal cell growth in mammals, especially humans.
WO2014128189A1 2-aminopyrimidine derivatives for the treatment of viral infections This invention relates to 2-aminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
US7091214 Immonomoderators; viricides; anticancer agents Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
CN103565776A Stable lurasidone capsule pharmaceutical composition The invention discloses a lurasidone capsule pharmaceutical composition and a preparation method thereof. The lurasidone capsule pharmaceutical composition is characterized in that a formula for preparing 1000 pills comprises 1-6 g of lurasidone, 40-240 g of lactose (Meggle C80), 10-60 g of microcrystalline cellulose (JRS 12), 5-30 g of cross-linked sodium carboxymethyl cellulose and 0.2-1.2 g of magnesium stearate. The invention also relates to a preparation method for the lurasidone capsule pharmaceutical composition. The method includes drying raw materials and auxiliary materials respectively at 80 DEG C for 3 h, mixing uniformly according to an equal proportion, and filling capsules. The lurasidone capsule prepared by the formula and the preparation method has good fluidity, good dissolution rate, small filling-amount difference, high biological utilization rate and good curative effects.
CA2307163C Process for stereoselective synthesis of prostacyclin derivatives An improved method is described for making 9-deoxy-PGF1-type compounds of the general formula:(see above formula) In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.
CN1569878A siRNA nucleic acid sequence for SARS coronavirus causing gene and its pharmaceutical use The invention discloses a small interfering RNA (siRNA) sequence targeting coronary virogene of Severe Acute Respiratory Syndrome (SARS), which is compatible with the nucleic acid sequence on specific positioning spots on the SARS coronavirus gene, thus can block the reproduction or expression in human body or animal body and achieve the goal of treating the disease. The invention also relates to the target sequence for resulting siRNA attacks on SARS coronavirus, the medicinal composition containing the siRNA sequence and early stage sequence, and its pharmaceutical use.
WO2008047951A2 An alzheimer' s disease progression inhibitor containing heterocyclic compound An Aizheimer's disease progression inhibitor comprising a heterocyclic compound having the general formula (I).
US20080287516 Phenyl-Substituted Pyrrolidones The present invention relates to phenyl-substituted pyrrolidones and compounds related to phenyl-substituted pyrrolidones. One use of these compounds is for the inhibition of viruses, e.g., HIV. The invention further relates to methods of malting these compounds, methods of identifying the efficacy of these compounds, and methods of using these compounds to inhibit or prevent HIV infection and related disease states such as AIDS.
EP1874730A1 Substituted butyrophenone derivatives The present invention relates to a central nervous system-acting substituted butyrophenones. These compounds are useful in antipsychotic medications for psychosis, including schizophrenia, but especially for L-DOPA-induced psychosis, while having low or no risk of eliciting extrapyramidal side effects, hyperprolactinemia or tardive dyskinesia.
CN103083333A Application of tanshinone IIA in preparation of medicine for treating malassezia induced skin disease The invention discloses an application of tanshinone IIA in preparation of a medicine for treating malassezia induced skin disease, and specifically provides the application in overmuch scurf, atopic dermatitis, seborrheic dermatitis and seborrheic dermatitis which are induced by tanshinone reproduction.
CN103272241A Target SERS (Surface Enhanced Raman Scattering) probe with pH-sensitive drug release characteristic, and preparation method thereof The invention discloses a target SERS (Surface Enhanced Raman Scattering) probe with pH-sensitive drug release characteristic. The probe comprises a Raman molecule-labeled gold nanoparticle core, a silicon dioxide intermediate layer, a mesoporous silica layer, a pH-sensitive polymer layer, a shell layer and a target ligand on the surface of the shell layer sequentially from inside to outside, the pH-sensitive polymer layer is a chitosan/polymethylacrylic acid layer, and the target ligand is transferrin. The invention further discloses a preparation method for the SERS probe. The probe and the preparation method thereof have the advantages that a pH-sensitive drug release system is combined with SERS, and the target ligand is connected with target tumor cells; the diffusion and release speed of drug in nano-particles can be regulated and controlled according to the pH value of the environment; the tracking on the nano-drug carrier particles can be more accurate through SERS signals in nano-drug carriers; and the target ligand is used for increasing the accumulation of drug in tumor parts, and increasing the transfer of drug in tumor cells.
EP2586781A1 Novel condensed pyridine or condensed pyrimidine derivative, and medicinal agent comprising same The present invention relates to provision of a novel compound that has an activity of promoting insulin secretion from pancreatic β cells and thus is useful as a prophylaxis and/or therapeutic agent for diseases caused by hyperglycemia such as diabetes mellitus, and the compound represented by the following formula (1): wherein one of A and B represents a nitrogen atom and the other represents a nitrogen atom or CR10, X represents an oxygen atom, a sulfur atom or - (CH2)n-N(R12) -, Y represents an oxygen atom, a sulfur atom or -N(R13)-, and R1 to R9 each represent a hydrogen atom or another substituent, or a salt thereof, or a solvate of the compound or the salt.
US20110195156 Sustained release beads and suspensions including the same for sustained delivery of active ingredients Sustained-released beads providing active ingredients over an extended period of time to an individual orally ingesting the sustained release beads. The sustained-release beads can be part of a suspension wherein the sustained-release beads are suspended and evenly dispersed in the suspension. Binding agents are used to form the structural framework of the sustained released beads and retain the active ingredients without chemical or electrical bonding. The components of the dispersion medium are GRAS designated, making the suspension suitable for use as a food product.
CN102911075A New crystal form I of agomelatine sulfate and preparation method thereof The invention relates to a new crystal form I of an agomelatine sulfate and a preparation method thereof. The preparation method of the crystal form I comprises the steps of heating and dissolving the agomelatine sulfate in a soluble solvent, slowly dripping into an anti-solvent to precipitate crystals, filtering and vacuum drying to obtain the crystal form I. The soluble solvent can be selected from alcohol and amide, and the anti-solvent can be selected from ester and alkane.
US20100160381 RAF Inhibitors for the Treatment of Thyroid Cancer The invention relates to the use of an Raf inhibitor for the manufacture of pharmaceutical compositions for the treatment of thyroid cancer, more specifically papillary thyroid cancer (PTC); the use of a Raf inhibitor in the treatment of thyroid cancer, more specifically PTC; a method of treating warm-blooded animals including mammals, especially humans, suffering from thyroid cancer, more specifically PTC, by administering to a said animal in need of such treatment a dose effective against said disease of an Raf inhibitor. The invention also relates to the use of a Raf inhibitor in combination with a platin compound for the treatment of thyroid cancer, more specifically papillary thyroid cancer.
US20100261739 Method of Treating Non-Small Cell Lung Cancer A method of treating non-small cell lung cancer (NSCLC), and especially NSCLC that has metastasized to brain is disclosed.
US20100183713 Gastrointestinal-specific multiple drug release system The present invention provides compositions and methods for the multiple release of a drug in the gastrointestinal tract of a subject through the use of an oral multiple drug release system. The system provides site-specific release of the drug to both the small intestine and the colon in the form of multiple controlled doses for long-lasting efficacy, thereby reducing the drug dosing frequency.
US20120087979 Extended-release oral dosage forms for poorly soluble amine drugs Oral dosage forms for poorly soluble amine drugs are provided. Such dosage forms include an ionizable compound such as an organic acid, an amphiphilic polymer and a release rate-controlling membrane. Such dosage forms allow for the consistent release of the active agent in both gastric pH conditions and in the intestine. Methods of making such dosage forms are also provided.
CN102133230B Compound mactra veneriformis organic calcium preparation and preparation method thereof The invention discloses a compound mactra veneriformis organic calcium preparation and a preparation method thereof. The organic calcium preparation consists of 90 to 95 parts of mactra veneriformis organic acid calcium, 0.1 to 0.5 part of vitamin B2, 0.5 to 1 part of vitamin D3 and 1 to 5 parts of casein phosphate peptide. The organic acid calcium is prepared from mactra veneriformis shells by the steps of calcining at a high temperature, crushing, dissolving in hydrochloric acid, removing acid insoluble matters, precipitating by adding sodium carbonate, performing suction-filtration, drying, performing secondary calcining, reacting with organic acid in water, standing, suction-filtering, drying and crushing. By a great number of experimental researches, after being scientifically combined with the vitamin B2, the vitamin D3 and the casein phosphate peptide, mactra veneriformis organic calcium has full nutrients and higher calcium absorptivity; the preparation method of the mactra veneriformis organic calcium is stable in process and high in operability; particularly, the purity of the prepared organic acid calcium can be over 99 percent; and the organic acid calcium contains trace elements required by human bodies such as Fe, Cu, Zn and the like, has low content of heavy metal, and meets the national food standards.
CN1594300A Compounds against influenza virus and their preparing process and application The invention relates to a formula I compound / or its pharmaceutically available salt or solvate, and their preparing process and use thereof, wherein the neuraminidase restaining agent has appreciable inhibitory action for influenza virus, thus can be used in preparing medicament for treating influenza diseases.
US20100175796 Anti fungal and anti-microbial protection for storage items and protective covers Anti fungal and anti-microbial protection for storage items and protective covers.
US20090162383 Method for designing vaccines against constantly mutating pathogens A unique method is disclosed for identifying and replacing surface amino acid residues of a protein antigen that reduces the antigenicity of the putative immunodominant epitopes of the antigen and makes all the accessible regions of the molecule essentially antigenically equivalent, so that the antibody response will be directed against more parts of the molecule and not mainly against the erstwhile immunodominant epitopes. The method will simultaneously change the antigenicity of the molecule and preserve its structure. The method is useful in the design of molecules useful for immunization, for example, as vaccines, or for the generation of therapeutic antibodies, against constantly mutating pathogens. It is also useful in the design of molecules useful for immunization against pathogens that had been intentionally mutated so as to render those pathogens able to infect erstwhile immune individuals.
CN102311430A Novel crystalline state of iloperidone and preparation method thereof The invention discloses a novel crystalline state of iloperidone and a preparation method thereof. The crystalline state is a stable high-purity iloperidone crystalline state form, has the characteristics of easiness, convenience and practicability in operation and high adaptability to industrial mass production, and is particularly suitable to be prepared into a medicinal composition for clinical use.
WO2009040456A1 Novel chemotherapeutic agents for treating cancer The compounds of formula (I) where: R1, R2, R3 and R4 are independently H, or a radical selected from hydroxyl; -OR; and -OCOR; where R is a radical selected from (C1-C4)-alkyl, phenyl, -(CH2)n-phenyl with n =1 - 4, and a radical derived from the above-mentioned with benzene rings, by means of a mono-, di- or tri-substitution in the benzene rings thereof; the substitutes being a radical selected from halogen, (C1-C4)-alkyl, (C1-C4) alkoxyl and trifluoromethyl, R4 also includes halogen, and R1, R2 and R3 also include O; the broken line is a single or double bond, with the condition that: a) when the broken line is a simple or double bond, then R1, R2 and R3 have the above-mentioned meaning except for O, and b) when the broken line is a double bond, then R1, R2 and R3 are independently O, have proven to be active against a number of cancer cell lines, in particular against leukaemia.
US20080262096 Squaric Acid Derivatives Novel squaric acid compounds of the formula (I), in which R, R1, R1′, R2 and X have the meanings indicated in Claim (1), are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.
US20090029983 Novel heterocyclic compounds having anti-hbv activity This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to pharmaceutical compositions comprising thienopyridines and to the use of such compositions to treat Hepatitis B and other diseases.
EP2178899A1 17beta-cyano-18a-homo-19-nor-androst-4-ene derivative, use thereof and medicaments containing said derivative The 17ß-cyano-18a-homo-19-nor-androst-4-ene derivatives of the present invention have gestagenic activity. They have the general chemical formula (1), in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, wherein R is hydrogen or C1-C4 alkyl, R4 is hydrogen or halogen and in addition either: R6a, R6b together form methylene or 1,2 ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4 alkyl, C2-C3 alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together either form methylene, or are omitted, whereby a double bond is formed between C6 and C7, R9 and R10 are hydrogen, or are omitted, whereby a double bond is formed between C9 and C10, R15 and R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4 alkyl and aIIyI, at least one of the substituents R4, R6a, R6b, R7, R15, R16 and R17 not being hydrogen, or R6b and R7 being omitted, whereby a double bond is formed between C6 and C7, or are omitted, whereby a double bond is formed between C1 and C2. The derivatives also comprise the solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts of the aforementioned substances.
CN103374007A Salt of dihydrochelerythrine derivative The invention relates to fumarate or pharmacological acceptable solvates of dihydrochelerythrine and derivatives of the dihydrochelerythrine as well as an application of the fumarate or pharmacological acceptable solvates to the preparation of drugs for treating hepatitis B.
CN102940810A Medicinal preparation for treating urinary calculi The invention relates to a medicinal preparation for treating urinary calculi. The medicinal preparation for treating urinary calculi is prepared from 10 to 15g of atractylodes rhizome, 20 to 30g of yellow ginseng, 20 to 30g of milkvetch root, 10 to 15g of achyranthes root, 10 to 15g of montmorillonite and 15 to 20g of coix seed. The medicinal preparation for treating urinary calculi has the advantages of high stone decomposition and expelling rate, good curative effect, short treatment course and no side-effect.
EP2228369A1 Pyrazole derivatives as protein kinase modulators The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
CN102754831A Formula of propolis, balsam pear and ginkgo leaf composite preparation with function of reducing blood sugar The invention provides a formula of a propolis, balsam pear and ginkgo leaf composite preparation with a function of reducing blood sugar. The formula comprises the following components in parts by mass: 50 to 60 parts of propolis, 60 to 70 parts of balsam pear extract, 45 to 55 parts of ginkgo leaf extract, and 0.1 to 0.3 part of chromium picolinate. The formula of the propolis, balsam pear and ginkgo leaf composite preparation with the function for reducing the blood sugar is used for assisting in reducing the blood sugar, and has a good effect and low side effect.
WO2010072105A1 A enteric formulation of duloxetine and its core and prepration method An enteric formulation of duloxetine, its core and preparing method thereof are disclosed. The core comprises duloxetine or its salt and pharmaceutically acceptable excipients. The excipients include water-soluble hot melt materials selected from PEG, poloxamer, polyoxyl (40) stearate or their mixture. Based on the total weight of the core, the amount of water-soluble hot melt materials is 10%~40% and the amount of duloxetine or its salt is 15~60%. The core material is prepared by hot melt process.The enteric formulation comprises the core, a separating layer and an enteric layer.
US20090012039 Use of methylcobalamin nasal spray to treat disorders A method of treating a disorder by nasally administering methylcobalamin, with or without folinic acid. The disorders addressed are: a) attention deficit hyperactivity disorder (ADHD); b) anxiety, depression, stress and chronic stress; c) socialization problems, mood problems, behavior problems, memory problems; d) dislexia, depth perception problems, color viewing problems, visual and auditory processing problems, light modulation problems, night vision problems; e) speech problems such as finding words, apraxia, and articulation problems, sleep regulation problems, eye or muscle movement problems; and f) chronic fatigue problems, digestion problems, sensitivity to chemicals, viral infection, inflammatory conditions such as rheumatoid arthritis, sciatica, and fibromyalgia, asthma, irritable bowel, colitis, tinnitus, migraines, nail biting, autoimmune problems. In some embodiments, the disorders that are particularly addressed are ADHD, anxiety, stress and chronic stress, and irritable bowel.
US20130079294 Extracts and isolated flavonoids from euphorbia cuneata useful as anti-ulcer agents The present invention relates to flavonoids isolated from Euphorbia cuneata, a method for their isolation, extracts from Euphorbia cuneata and a pharmaceutical composition comprising the flavonoids or the extracts or both of them for a use as anti-ulcer agent.
WO2010066815A2 Encapsulating system for cest imaging with chelate q greater than or equal to 2 The present invention relates to the use of a CEST contrast agent in a method of CEST imaging, wherein the contrast agent is a composition comprising an encapsulating system ES encapsulating at least one CEST agent, wherein the at least one CEST agent is constituted of a monomeric chelate of a chelate of q ≥ 2 type, or of a multimer of monomeric chelates of q ≥ 2 type, and wherein said chelate is free inside the encapsulating system.
WO2014135423A1 N-heteroaryl substituted aniline derivatives as hcv-antivirals The present invention discloses compounds of Formula (I): wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
US6861420 N-substituted 1,2,4,5-tetrahydro-1H-benzo[d]azepine compounds The present invention provides compounds of Formula I: wherein X, R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula I.
CN102716123A Compound preparation for treating IgA nephropathy The invention discloses a compound preparation for treating IgA nephropathy. The compound preparation for treating the IgA nephropathy consists of the following components in parts by weight: 5-15 parts of sartan medicine and 50 parts of probucol. The compound preparation is obvious in curative effect on slight proteinuria IgA nephropathy, moderate proteinuria IgA nephropathy and severe proteinuria IgA nephropathy. Shown by experimental results, the compound preparation is superior to single reagents, can be used for treating the IgA nephropathy better and is small in side effect.
CN101283998A Application of bromine phenolic compound in preparing the medicine for curing the malignancy The invention relates to a drug for treating malignant tumors, particularly to an application of bromophenols in preparing drugs for treating malignant tumors. The bromophenols and sodium salts, ester, ether and other derivatives thereof have good inhibitory effect on protein tyrosine kinase, and can be used for treating and preventing malignant tumors with high expression of C-kit receptor.
CN103536897A Compound for inhibiting aggregation of amyloid polypeptide as well as preparation method and application thereof The invention discloses a compound for inhibiting aggregation of amyloid polypeptide as well as a preparation method and application thereof. The compound is prepared from a short peptide inhibitor and an adjuvant according to a molar ratio of (1:5) to (10:1), wherein the short peptide inhibitor is selected from segments of 3-10 amino acids of beta-amyloid polypeptide, mutants and derivatives thereof; the adjuvant is selected from a nitrogenous heterocyclic compound and derivatives thereof; according to the compound, the short peptide inhibitor and the adjuvant are dissolved into a buffer solution according to the molar ratio of (1:5) to (10:1), so as to prepare a mixed solution; the final concentration of the short peptide inhibitor is 10-100 muM; the compound is prepared in an incubation manner; the compound is used for preparing a drug for inhibiting the toxic action of the amyloid polypeptide on a cell or used for preparing a drug for treating and/or preventing a disease associated with the amyloid polypeptide. The invention discloses interaction of molecules and the amyloid polypeptide in the molecular level; an effective method is provided for research on an interaction mechanism of drug molecules and the amyloid polypeptide.
WO2014063054A1 Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and/or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.
CN1837218A N2,N4-disubstituted pyrazolo [4.5-e][1,2,4] thiadiazine derivatives and use thereof The invention relates to N2,N4-disubstituted pyrazolo [4.5-e][1,2,4] thiadiazine derivatives, wherein the derivative has a structural formula disclosed in the specification, R1, R2 are benzyl, p-bromobenzyl, m-bromobenzyl, o-bromobenzyl, p-cyanobenzyl, ortho-cyanobenzyl, m-cyanobenzyl, 2,4-dichlorobenzyl, p-chlorobenzyl, m-chlorobenzyl, and p-methylbenzyl. The preparing process comprises using 1-methyl-5-sulfonamide-4-pyrazole aminobenzoafe as the starting raw material, carrying out hydrogenolysis, diazotization, Curtius rearrangement reaction and N2, N4-dialkylation. The derivative has the activity of part of HIV-1 reversetranscriptase inhibitor, thus can be used for the preparation of anti-AIDS medicaments.
EP1163234B1 Pharmaceutical formulations with improved aqueous solubility A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.
CA2231509C Protein tyrosine kinase inhibitors for treating osteoarthritis Disclosed is a method of treating an individual or animal with osteoarthritis. The method comprises administering to the individual or animal a therapeutically effective amount of a protein tyrosine kinase inhibitor.
WO2008126363A1 Drug for preventing and/or treating fatty liver or nonalcoholic fatty liver disease A drug for preventing and/or treating fatty liver or nonalcoholic fatty liver disease with little side effect which contains a polyprenyl compound (for example, 3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid) as the active ingredient.
EP2521721A1 3-(3-aminopiperidin-1-yl)-5-oxo-1,2,4-triazine derivates as dipeptidyl peptidase iv(dpp-iv) inhibitors Provided are 3-(3-aminopiperidin-1-yl)-5-oxo-1,2,4-triazine derivates as dipeptidyl peptidase IV(DPP-IV) inhibitors, pharmaceutical compositions thereof, and methods of use thereof.
WO2013102195A8 Compositions, synthesis, and methods of using phenylcycloalkylmethylamine derivatives The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
CA2526862A1 Methods of diagnosing, prognosing and treating breast cancer The protein pRb2/p130 represses expression of the ER-.alpha. gene. Blocking pRb2/p130 expression or altering ER-.alpha. gene methylation to alter pRb2/p130 complex binding allows transcriptional activity of the ER-.alpha. gene to be restored. Detecting and regulating the methylation state of the ER-.alpha. gene, optionally together with detecting and regulating pRb2/p130 multimolecular complexes bound to the ER-.alpha. gene promoter, allows estrogen-insensitive breast cancer cells to be identified, so that an accurate prognosis can be obtained and an appropriate course of treatment administered. Also, inhibiting pRb2/p130, or altering the methylation pattern of the ER-.alpha. gene by targeting DNMT 1 I n the pRb2/p 130-E2F4/5-HDAC 1-DNMT1-SUV39H1 complex, allows estrogen-insensitive breast cancer cells to be converted to estrogen-sensitive breast cancer cells. Estrogen-sensitive breast cancer cells which are generally more susceptible to current anti-cancer treatments.
WO2008109996A1 Assessing chemotherapy resistance of colorectal tumors by determining sparc hypermethylation Hypermethylation of the SPARC promoter is identified as a mechanism for repressing SPARC gene in cancer resulting in resistance to therapy. The restoration of SPARC expression with demethylating agents, such as 5-Aza-2'deoxycytidine, is shown to enhance chemosensitivity. The invention provides a mechanism of limiting the number of patients exposed to toxicity of demethylating agents by targeting its administration to the subset of patients with hypermethylation of the SPARC promoter.
CN103405453A Application of Chukrasone A in medicaments for treating pancreatic carcinoma The invention discloses an application of Chukrasone A in preparing medicaments for treating pancreatic carcinoma, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT(3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluation finds that the Chukrasone A also has a significant inhibitory effect on the growth of human pancreatic carcinoma cell strains PANC-1 and BXPC-3. Therefore, the Chukrasone A can be used for preparing anti-pancreatic carcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating pancreatic carcinoma provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to pancreatic carcinoma cells.
CN102617480A Di-(hetero)aryl-substituted tertiary amine compounds, preparation method thereof and antitumor application thereof The invention relates to di-(hetero)aryl-substituted tertiary amine compounds with the general formula of formula I or pharmaceutically acceptable salts thereof, a preparation method thereof, pharmaceutical compositions containing the compounds, and an application of the compounds in the preparation of antitumor drugs. In the formula I, X, Y, Z, Ar, L, and R1-R4 are defined in the specification.
CN103435672A Structure and synthesis of novel nucleoside phosphate prodrug containing substituted benzyl The invention describes a phosphate structure containing substituted benzyl, wherein the phosphate structure is shown as a formula (I) and a formula (II). The phosphate structure can be used as prodrugs for various nucleoside analogues including non-cyclic nucleoside, carbon-cyclic nucleoside, furan-cyclic nucleoside and the like, and enhance bioactivity of nucleoside compounds, and thus the structure can be applied in treatment for virus infections and cancers.
EP2727598A1 Biological inorganic compound complex having reduced oxygen and high reducing ability Object; To provide a biological inorganic compound complex which has few adverse side-effects can treat Graves' disease within a short period of time and suppress the influence of active oxygen (oxidization) which has been believed to be one of causes of other disease to achieve thereby a pharmacological effect, a cosmetic effect, an animal-or-plant-growing effect and an environment-improving effect, which has reduced oxygen and a high reducing ability but cannot be produced by a synthetic chemical technique. [Solution] To provide an inorganic composite compound having reduced oxygen and a high reducing ability, which comprises elements having a positive atomic valence of a plant-derived component and a sulfur compound. Selected Fig. None
US7781468 peroxisome proliferator-activated receptor (PPAR) agonists such as (2S)-3-{-4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)-ethoxy]-phenyl}-2-(3-phenyl-acryloylamino)-propionic acid, used for the treatment of hyperglycemia, dyslipidemia, non-insulin dependent diabetes and hyperlipemia The present invention relates to a compound of formula I, racemates, optically active isomers, or pharmaceutically acceptable salts or solvates thereof, and a pharmaceutical composition comprising the compound, the various radicals in the formula I are the same as defined in the claims. The present invention also relates to a process for preparing the compound of formula I and use of said compound in the preparation of a medicament for the treatment of hyperglycemia, dyslipidemia, type II diabetes mellitus including associated diabetic dyslipidemia
EP2633856A2 ATP citrate lyase inhibitors for treating cancer Methods of treating individuals identified as having cancer using ATP citrate lyase inhibitor and/or tricarboxylate transporter inhibitor are disclosed. Methods of inducing apoptosis in cancer cells using an ATP citrate lyase inhibitor and/or tricarboxylate transporter inhibitor are disclosed. Methods of treating an individual who has cancer comprising the steps of identifying the cancer as having a high rate of aerobic glycolysis, and administering an ATP citrate lyase inhibitor and/or tricarboxylate transporter inhibitor are disclosed. Methods of treating individuals who have cancer using compounds that inhibit the expression of ATP citrate lyase or tricarboxylate transporter are disclosed. Methods of identifying a compound with anticancer activity are disclosed.
US20080021061 Tetrahydropyranyl Cyclopentyl Tetrahydropyridopyridine Modulators of Chemokine Receptor Activity Compounds of Formula I: (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
WO2010068500A2 PROGESTATIONAL 3-(6,6-ETHYLENE-17b-HYDROXY-3-OXO-17a-PREGNA-4-ENE-17a -YL) PROPIONIC ACID g-LACTONES Described herein are 3-(6,6-ethylene-17β-hydroxy-3-oxo-17α-pregna-4-ene-17α-yl) propionic acid γ-lactone derivatives having progestational and aldosterone antagonistic activity. Also described herein are methods of preparing and using these novel compounds.
WO2014036556A3 Drug delivery systems and methods for treatment of prostate disease comprising gemicitabine Methods, devices, and medicaments that include gemicitabine are provided for use in the treatment of the prostate disease by locally administering gemicitabine into the bladder of a patient to achieve a sustained concentration of the drug in urine in the bladder sufficient to produce a therapeutic concentration of the drug in the prostate. Gemicitabine may be delivered into the bladder from an intravesical drug delivery device inserted into the bladder, wherein the device continuously releases the drug into the urine in the bladder over an extended period of hours or days.
US20080300275 Novel Benzothiazolone Derivatives The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4, R5, R6, R7, R7a, R7b, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
CN102961331A Iodine-chitosan solution formula and preparation method thereof The invention discloses an iodine-chitosan solution formula and a preparation method thereof. The raw materials of the iodine-chitosan solution include iodine-chitosan, glacial acetic acid, polysorbate-20, glycerol, potassium iodate and purified water. The preparation method comprises the following steps that: (1) the materials are weighed; (2) the glacial acetic acid, polysorbate-20, glycerol and purified water are added into the iodine-chitosan and uniformly mixed to totally dissolve; (3) the potassium iodate is dissolved by the purified water and then added into the materials and uniformly mixed; (4) the purified water is added inside the materials to reach 100 percent and the materials are uniformly mixed; and (5) the mixture is filtered, filled, packaged to obtain the iodine-chitosan solution. In the iodine-chitosan solution, the iodine-chitosan plays the role of disinfection and sterilization, the glacial acetic acid plays the role of pH value adjustment and synergetic solubilization, the polysorbate-20 plays the role of solubilization, the glycerol plays the role of blending and moisture retention, the potassium iodate plays the role of a stabilizer, and the iodine-chitosan plays the role of disinfection; and the iodine-chitosan solution can be used for skin disinfection of operation sites or injection sites and auxiliary treatment of small cuts, and also can be used for washing treatment of vagina inflammation and treatment and disinfection of oral diseases.
CN103565745A Neuroprotective liposome compositions and methods for treatment of stroke Methods for the treatment of stroke, such as stroke of undetermined origin, by administration of xenon (Xe)-loaded liposome compositions are provided. In some aspects, Xe is encapsulated in echogenic liposomes and release of Xe can be enhanced by application of ultrasound stimulation. Compositions for use in treating stroke, such as liposomes loaded with Xe or Xe in combination with H2 or H2S, are also provided.
WO2011011420A3 3, 4-methylenedioxyphenyl inhibitors of gaba aminotransferase and/or gaba reuptake transporter inhibitor The present invention relates to new 3,4-methylenedioxyphenyl inhibitors of GABA aminotransferase activity and/or GABA reuptake transporter activity, pharmaceutical compositions thereof, and methods of use thereof. Formula (I)
EP2491929A1 Use of Nifuratel to treat infections caused by Clostridium species The present invention is directed to the use of nifuratel, or a physiologically acceptable salt thereof, to treat infections caused by bacteria species of the genus Clostridium. The invention is further directed to the use of nifuratel to treat Clostridium difficile infection (CDI) and in particular Clostridium difficile associated diarrhoea (CDAD).
CN1830421A Clindamycin phosphate foamable composition and its preparation method A clindamycin phosphate foam for treating gynopathy is prepared through dissolving clindamycin phosphate in water, adding sodium laurylsulfate, stirring, adding distilled water, stirring, filling it in hand-pressing net-type foam emulsion generator, and hand pressing to generator foam.
DE102005057408A1 New sulfamoylsulfonate prodrugs e.g. useful for protecting red blood cells from attack by parasites or for hormone replacement therapy, female fertility control or treating hormone-associated diseases Sulfamoylsulfonate prodrugs (I) are new. Sulfamoylsulfonate prodrugs of formula (I) are new. Drug-O-SO2-X-SO2NH2 (I) X : 1-12C alkanediyl, 1-5C perfluoroalkylene, 3-8C cyloalkanediyl, arylene, heteroalkanediyl, 1-4C alkanediylaryl, (1-4C)alkanediyl(3-8C)cycloalkyl or (3-8C)cycloalkanediyl(1-4C)alkyl; Drug : a pharmaceutical agent capable of forming a sulfonate through an OH group. Independent claims are also included for: (1) pharmaceutical composition comprising a prodrug (I) and another active agent; (2) a process for preparing (I). - ACTIVITY : Antiparasitic; Protozoacide; Gynecological; Cytostatic; Antiinflammatory; Antiallergic. - MECHANISM OF ACTION : None given.
CN101092408A Lactone compound of sweetsop connected through amido bond, synthetic method and application This invention relates to an acetogenin compound linked by amide bonds, its synthesis method and its application. The acetogenin compound is an optically active or racemized compound, whose structural formula is shown in this invention, wherein, Y is C6-20 alkyl; n is 0-3; m is 7-19; R1, R2, R3 and R4 are the same or not, and are H or C1-10 alkyl; when n is 0-2, R3 and R4 are H, Cl, C1-10 alkyl or combined to form fiver-, six- or seven-membered ring shape; when n is 0, R1 and R2 are C1-10 alkyl or combined to form fiver-, six- or seven-membered ring shape. The acetogenin compound has high anticancer activity, and IC50 (mu.M) is lower than 0.04 to breast cancer (MDA-MB-435S). The can be manufactured into anticancer drugs. The synthesis method is simple, and suitable for industrial production.
WO2008142140A2 Novel 2,3-diamino-quinazolinone derivatives and their medical use This invention relates to novel 2,3-diamino-quinazolinone derivatives having medical utility, to use of the 2,3-diamino-quinazolinone derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2,3- diamino-quinazolinone derivatives of the invention, and to methods of treating a disord disease or a condition of a subject, which disorder, disease or condition is responsiv to activation of KV7 channels. A 2,3-diamino-quinazolinone derivative of Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically-acceptable addition salt thereof, or an N-oxide thereof.
WO2010055170A1 Pyrimidinium derivatives for use in the treatment or prevention of diabetes The present invention relates to methods and compositions for preventing or treating diabetes. The invention in particular discloses compounds according to formula (I) for use in the prevention and treatment of type II or I diabetes.
US20080317885 Compositions and Methods for Treating and Preventing Inflammatory and/or Degenerative Processes in Humans and Other Animals Disclosed are compositions useful for treating Alzheimer's disease, atherosclerosis, arteriosclerosis, osteoarthritis and other degenerative joint diseases, Huntington's chorea, Parkinson's disease, optic atrophy, retinitis pigmentosa, macular degeneration, muscular dystrophy, aging-associated degenerative processes, asthma, dermatitis, laminitis, pemphigoid, pemphigus, reactive airway disease (e.g., COPD, IAD), inflammatory bowel disease (e.g., Crohn's disease, ulcerative colitis), multiple sclerosis, rheumatoid arthritis, periodontal disease, systemic lupus erythematosus, sarcoidosis, psoriasis, type I diabetes, ischemia-reperfusion injury, chronic inflammatory diseases, geriatric wasting, cancer cachexia, cachexia associated with chronic inflammation, sick feeling syndrome, and other inflammatory and/or degenerative diseases, disorders, conditions, and processes in humans and other animals. In one embodiment, the compositions include at least 4 of the following: a MMP1 inhibitor, a MMP2 inhibitor, a MMP3 inhibitor, a MMP7 inhibitor, a MMP9 inhibitor, an ADAMTS-4 inhibitor, a MMP13 inhibitor, and a MMP14 inhibitor. In another embodiment, the compositions include a curcuminoid, a polymethoxylated flavone, a catechin, and a boswellic acid.
WO2009064747A2 4(-3-(-2-(phenyl) morpholino)-2-oxopyrrolidin-1-yl)-n-(thiazol-2-yl) benzenesulfon amide derivatives and related compounds as modulators of ion channels for the treatment of pain The present invention relates to heterocyclic derivatives of formula I useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, like, e.g. pain., (I) or a pharmaceutically acceptable salt thereof, wherein, independently for each occurrence: ring Z is a thiazole or thiadiazole optionally substituted with 0-2 occurrences of R; V is CH2, NH, O, or S; and R, R1, R2, and R3 are hydrogen, C1-C6 aliphatic, aryl, C3-C8 cycloaliphatic, halo, CN, NO2, CF3, OCF3, OH, NH2, NH(C1-C6 aliphatic), N(C1-C6 aliphatic) 2, COOH, COO(C1 -C6 aliphatic), O(C1-C6 aliphatic), CHF2, or CH2F.
US7419804 CASH (Caspase Homologue) with death effector domain, modulators of the function of FAS Proteins capable of modulating or mediating the function of MORT-1 are disclosed. Also disclosed are DNA sequences encoding these proteins, the recombinant production of these proteins as well as their use.
US20080267967 Modulation of cd200 receptors The present invention relates to CD200 receptor isoforms and modulators thereof and their use in methods of immune modulation and pharmaceutical compositions.
US20110091534 Compositions comprising polymeric micelles for drug delivery The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same.
US20100068314 Herbal composition for treating cd33+ acute and chronic myeloid leukemia and a method thereof A method of treating CD33+ acute and chronic myeloid leukemia in animals including humans, using fraction nos. 1 and 9 obtained from water:methanol fraction by column chromatography, with ratio of water and methanol ranging between 1:5 to 5:1, wherein said water:methanol fraction is obtained from the polar extract of Piper betel by HPLC, with retention time of 3.6 and 24.0 minutes respectively, with said fractions used both individually, and in combination.
CN102626405A Application of paclitaxel in preparation of medicament for treatment of EGFR-TKI acquired resistance The invention relates to application of paclitaxel in preparation of medicament for treatment of non small cell lung cancer EGFR-TKI (epidermal growth factor receptor-tyrosine kinase inhibitor) resistance. Lung cancer ranks the first in cancer incidence and mortality all over the world. Curative effects of Gefitinib and Erlotinib in NSCLC are often limited by acquired resistance, and currently known main mechanism of acquired resistance is due to mutation of second generation of EGFRT790M and acquired amplification of MET gene. The invention shows that when EGFR-TKI acquired resistance appears, paclitaxel may reverse the resistance. That is to say, non small cell lung cancer patients who generate acquired resistance from Erlotinib / Gefitinib treatment can reconsider the use of Erlotinib / Gefitinib treatment after chemotherapy with paclitaxel, so as to make the erlotinib / gefitinib continue to function; meanwhile, paclitaxel may also inhibit tumor, and thus play rotary resistance and synergism.
US20080182853 suppressing neuronal death; sudden loss of oxygen and/or energy loss, and degenerative diseases, such as Alzheimer's disease; Parkinson's disease; ischemic states The present invention relates to methods of suppressing neuronal death, such as is observed with ischemia-related diseases and disorders, including neuronal and cardiac conditions arizing from a sudden loss of oxygen and/or energy loss, and degenerative diseases, such as Alzheimer's disease to name just one. The methods involve the use of inhibitors that act primarily in a simultaneous manner on the cyclin-dependent kinases, CDK4 and CDK6.
CN101679293A Urocanic acid derivatives useful for the treatment of immune-related and inflammatory diseases The invention relates to derivatives of urocanic acid that have improved efficacy and/or tissue penetration properties. The invention further provides use of these derivatives in a medicament for modulating an immune-related disease in an individual. Imidazole derivative, or a salt thereof, selected from formulas 1, 2, 3.
US20050147633 Insecticidal amides with nitrogen-containing benzo-Fused bicyclic ring systems Disclosed are compounds of Formula I and compounds of Formula II (including all geometric and stereoisomers), N-oxides thereof and salts thereof, certain compositions comprising the compounds of Formula I and/or the compounds of Formula II and certain uses of those compounds and compositions for controlling invertebrate pests INSERT FORMULA I AND II HERE wherein A, B, J, R1, R2, R3, R4, M, M1 and n are as defined in the disclosure.
US20090169524 Composites and methods of preparation and use thereof The invention provides composites, methods for their preparation, composites prepared according to the methods, and methods for using the composites.
EP1861091A1 Compounds having lipid lowering properties There is provided a therapy for lowering the blood levels of a lipid selected from the group comprising LDL cholesterol, triglycerides, overall cholesterol and mixtures thereof, the therapy comprising the step of administering an effective amount of one or more phosphate derivatives of one or more electron transfer agents.
CN103006655A Application of chloroform extract of inonotus obliquus liquid fermentation product in preparation of antidiabetic drugs The invention relates to the application of a chloroform extract of inonotus obliquus liquid fermentation product in the preparation of antidiabetic drugs. The extract contains 19 types of compounds, and the combination of one or more types of the 19 types of compounds can be used for the preparation of dipeptidyl peptidase IV inhibitors and antidiabetic drugs.
CN103126983A Emulsion prepared by difluprednate crystal form I An emulsion prepared by a difluprednate crystal form I contains difluprednate used as active ingredients, one type or multiple types of oil, one type or multiple types of emulgator and water. The emulsion comprises, by weight, 0.01% to 0.1% of the difluprednate, 1% to 20% of the oil, and 1% to 10% of the emulgator. The emulsion prepared by the difluprednate crystal form I is characterized in that when the emulsion is prepared, the difluprednate adopted is the difluprednate crystal form I, wherein the X-ray powder diffraction of the difluprednate crystal form I has a characteristic peak when a diffraction angle 2theta is 8.9 degrees, 11.6 degrees and 17.6 degrees.
US20100197802 Skin dressings Improvements relating to skin dressing A skin dressing adapted, on activation, to generate one or more S-nitrosothiols by reaction between a thiol and a nitrate salt in the dressing, the skin dressing comprising a source of Cu2+, Zn2+ and/or Fe2+ ions for delivery of nitric oxide to a body site is provided.
WO2011023287A1 Use of faa and its derivatives in cosmetics and dermatology The invention relates to flavone acetic acid, its derivatives and its use in compositions, especially topical, cosmetic and/or personal care compositions, and compositions containing flavone acetic acid and/or its derivatives.
US20080280941 8-Phenoxy-Gamma Carboline Derivatives Compounds of Formula I and corresponding pharmaceutical compositions are disclosed.
WO2006075095A2 Use of purine derivatives as hsp90 protein inhibitors and for treatment of cancer The invention relates to the use of purine derivatives as Hsp90 protein chaperone inhibitors and more particularly the use thereof as inhibitors of the ATPase catalytic activity of the Hsp90 protein chaperone.
WO2012075020A1 Treatment of obesity using non-daily administration of 6 - 0 - (4 - dimethylaminoethoxy) cinnamoyl fumagillol The invention generally relates to methods of treating an overweight or obese subject, and treating overweight- or obesity-related conditions using non-daily administration of e.g, a MetAP-2 inhibitor.
US20110207814 Combination Therapy for Breast Cancer Treatment The present invention provides a novel treatment which features immune therapy in the context of the functions of MSCs as a novel approach to breast cancer treatment. By identifying and elucidating the role of MSCs in the behavior of breast cancer cells at metastatic sites and also at the primary region, this invention provides novel approaches for therapeutic intervention. More particularly, in the presence of MSCs a CXCR4 antagonist transitioned BCCs into cycling cells and conferred susceptibility to a chemotherapeutic agent. The proliferation of BCCs depended on the release of IL-1α and IL-1β from MSCs, but only if the CXCR4 antagonist uncoupled BCCs from MSCs.
EP1499309A1 Prevention and treatment of functional somatic disorders, including stress-related disorders Methods for the prevention or treatment of stress-related disor ders by administering a therapeutically effective amount of a dual serotonin/norepinephrine reuptake inhibitor to an individual under stress are described. A triple monoamine reuptake inhibitor for serotonin/noradrenaline/dopamine may also be administered to an individual at risk for a stress-related disorder. In a preferred embodiment the compound is milnacipran and is prophylactically administered at an effective amount to delay or prevent stress- related disorders in an individual at risk.
US7138403 2,4,5-trisubstituted thiazolyl derivatives and their antiinflammatory activity This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl or C1-6alkyloxy; polyhaloC1-4alkyl; C1-4alkyloxy; cyano; amino; aminocarbonyl; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H2N—S(═O)2—; mono- or di(C1-6alkyl)amino-S(═O)2; —C(═N—Rx)NRyRz; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-α and/or IL-12.
EP2432781A1 Salts of tiotropium with 10-camphorsulfonic acid The present invention relates to novel tiotropium salts with 10-camphorsulphonic acid of formula (I), its optical isomers or their mixtures, their monohydrates, their anhydrous crystalline forms and processes for the preparation thereof, as well as to pharmaceutical compositions containing the same and to the use of novel salts for the treatment of respiratory tract diseases. (I)
CN1576269A N- amino acid and producing process and use thereof The present invention relates to the synthesis of N-(1-desoxyglucitol-1-radical)-amino acid and its medicinal salt, relates to the use of N-(1-desoxyglucitol-1-radical)-amino acid and its medicinal salt as orally taken heavy metal exhausting preparation, and further relates to the use of medicine composition containing N-(1-desoxyglucitol-1-radical)-amino acid and its medicinal salt as orally taken heavy metal exhausting preparation.
CN102198264A Beta-defensin 15 of specific antibacterial peptides of rat epididymis and application thereof The invention relates to beta-defensin 15 of specific antibacterial peptides of rat epididymis and application thereof, in particular to Defb15 genes of rats or orthologous genes thereof or application of amino acid sequences of the Defb15 genes or the orthologous genes thereof in the preparation of medicines for regulating and controlling male fertility, the development of male contraceptive medicines and the preparation of medicines for diagnosing and treating male infertility and resisting genital tract infection. The invention also relates to a medicinal composition containing the genes or the amino acid sequences.
EP2119434A1 Use of heterosidic flavonoid derivatives for therapy of stem cell cancers The present invention relates to therapy of stem cell cancer and more specifically against acute myeloid leukaemia. The present invention more precisely deals with the use of heterosidic flavonoid derivatives and in particular rutin, or derivatives thereof for the treatment of stem cell cancer specifically acute myeloid leukaemia, for preventing tumor relapse in a patient and/or for preventing solid tumor metastasis in a patient.
CN102205006A External medicament for treating osteomyelitis and preparation method thereof The invention discloses an external medicament for treating osteomyelitis, which is prepared from the following Chinese medical raw materials in parts by weight: 15 parts of Chinese violet, 15 parts of evodia lepta, 10 parts of ampelopsis cantoniensis, 10 parts of cotton rose, 10 parts of pouzolzia zeylanica, 9 parts of ginseng, 10 parts of prepared calamine, 6 parts of prepared mastic, 6 parts of prepared arsenic, 1 part of musk, 2 parts of borneol, 5 parts of realgar, 6 parts of lead monoxide, 5 parts of calomel and 10 parts of stalactite. The external medicament disclosed by the invention has the advantages of high effect taking speed, high cure rate and low cost, is convenient to use, can not cause complications, and can ensure that the disease can not recur easily; and the effective rate is 95%, and the cure rate is 90%.
CN101953873B Medicament for treating furunculosis and preparation method thereof The invention discloses a medicament for treating furunculosis and a preparation method thereof. The medicament is characterized by comprising the following raw materials by weight: 3 to 4 grass spiders, 6 to 9 grams of alums, 15 to 20 grams of peeled cactus and a proper amount of flour and vinegar. The preparation method comprises the following steps of: mixing the grass spiders, the alums and the peeled cactus, mashing the mixture, adding a proper amount of flour, and blending the mixture into paste by using the vinegar to prepare the medicament. The medicament has the special effects of detumescence, pain relieving and inflammation diminishing, and relieves diseases for patients.
CN203263805U Resin container filled with antifungal drug composition The utility model provides a drug composition steadily containing the compounds and/or the salt compounds thereof shown by the formula (I), and provides a means for the market (in the formula (I), R1 and R2 in the formula respectively represent the hydrogen atom or halogen atom). The drug composition containing the compounds or the salt compounds thereof shown by the formula (I) is filled and stored in a resin container, wherein the container is colored by Munsell color coordinates in the range of hue (H) of 7.0Y-9.99Y or 7.0YR-9.99YR, the lightness (v) of 1.0-6.0 and the chroma of 0.5-7.5.
WO2014061808A1 Nutritional composition for gastrostomy-tube patients Provided is a nutritional composition that gastrostomy-tube patients, who are at significant risk for developing aspiration pneumonia and require careful risk management, can consume more safely with the development of aspiration pneumonia inhibited. That is, the present invention is a nutritional composition for administration to gastrostomy-tube patients, who require risk management for aspiration pneumonia, and is characterized by containing a protein source, a carbohydrate source, and a fat source, said protein source consisting only of amino acids.
WO2014160668A1 Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors The present invention provides compounds of Formula (I), or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
CN1736977A crystallized (+)-(1S,2S,3S,4R,5R)-1-amido-5-hydroxymethyl-N-2(1,3-dihydroxypropyl)-2,3,4-cyclohexanetriol and its preparation method The invention relates to a compound with novel crystallization shapes, i.e. (+)-(1S,2S,3S,4R,5R)-1-amido-5-hydroxymethyl-N-2-(1,3-dihydroxypropyl)-2,3,4-hexahydrophenol, which has stabilized shape and definite fusing point needed for large scale medicament synthesis or preparation.
EP1040101B1 Substituted 2-aryl-4-amino-chinazolines, method for the production and use thereof as medicaments The invention relates to inventive compounds of formula (I), wherein R?1, R2, R3¿ and Ar have the meanings cited in the claims. The inventive compounds are suitable for use in the production of medicaments, e.g. for prophylaxis and therapy of cardiovasular diseases such as hypertension, angina pectoris, heart failure, thromboses or arteriosclerosis. The compounds of formula (I) have a capacity for modulating endogenic production of cyclic guanosine monophosphate (cGMP) and are generally suitable for therapy and prophylaxis of pathological conditions linked to cGMP metabolism disorders.
WO2007139036A1 Compound for controlling endoplasmic reticulum stress, and pharmaceutical composition comprising the compound as active ingredient Disclosed is a compound for controlling the endoplasmic reticulum stress, which can show higher effect on endoplasmic reticulum stress which cannot be achieved by a conventional one. The compound is represented by the general formula I: wherein R1, R2, R3, R4, R5, R6, R7 and R8 independently represent a substituent selected from: a hydrogen atom; a halogen atom such as F, Cl, Br and I; a hydroxyl group; an alkyl group such as a methyl group, an ethyl group and a propyl group; an alkoxy group such as a methoxy group, an ethoxy group and a propoxy group; an aryloxy group such as phenoxy group; an acyloxy group such as acetyloxy group; a benzyloxy group; and the like.
WO2013144098A1 New indanyloxydihydrobenzofuranylacetic acid derivatives and their use as gpr40 receptor agonists The present invention relates to compounds of general formula (I), wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
CN102793695A New pharmaceutical application of 3-hydroxy fatty acid methyl ester and analogs thereof The invention discloses a new pharmaceutical application of 3-hydroxy fatty acid methyl ester and analogs thereof. The new application refers to an application in the preparation of medicaments for preventing and/or treating neurodegenerative diseases. Experiments show that the medicaments are easy to be absorbed by organisms, easy to pass through blood brain barriers and significant in efficacy, and side effects can be avoided. The medicaments can show an energy source for replacing glucose, promote the generation of ATP (adenosine triphosphate), enable cells to keep the normal oxidation reduction state, maintain the normal membrane potential of mitochondria and protect enzyme activity of a respiratory chain composite of mitochondria during cytological experiments. During water maze tests, the medicaments can obviously shorten the latent period during the learning process, significantly improve the learning ability and space exploration ability of model mice with Alzheimer's diseases, and further significantly improve the memory ability of the mice with cognitive disorder in the memory retention step. Nuclear magnetic resonance analysis of the brain shows that the medicaments can significantly inhibit the atrophy of hippocampal regions.
CN1894256A Method for preparing spironolactone compounds This invention relates to a process for making spirolactone compounds of general formula I, having an improved Ia/Ib ratio, according to the following shceme.
WO2008000745A2 Adenosine derivatives for the treatment of pain Compounds of formula (I) are disclosed. Their use as medicaments is described, in particular for the treatment of pain or inflammation. In said Fomula, when X=Y=Z=OH, R1 is OCH2CF2CF3, phenoxy (substituted with 3-(4-trifluoromethylphenyl), 3,4-dichloro, (3-trifluoromethyl,4-fluoro), (3-trifluoromethyl,4-chloro), (3-chloro, 4-cyano), or 3,5-bis(trifluoromethyl)), 1-piperazinyl(4-(3,4-dichlorophenyl)), phenyl (substituted with 3,4-dichloro, 3,5-difluoro, 3,5-bis(trifluoromethyl) or 3,4,5-trifluoro) or 2-benzofuranyl; or when X=Y=OH and Z=OMe, R1 is OCH3, OCH2CHF2, OCH2cyclopentyl, O-(2,5- difluorophenyl) or (S)-sec-butylamino; or when X=H and Y=Z=OH, R1 is n-hexylamino or cyclopentylamino; or when (IV) X=Z=OH and Y=H, R1 is cyclopentylamino;or a pharmaceutically acceptable salt thereof.
EP1040098B1 Integrin receptor antagonists The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αξβ3, αξβ5, and/or αξβ6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
WO2011087187A1 Composition for protecting fetal nerve cells comprising vitamin c The present invention relates to a composition which can protect fetuses from nerve damage caused by alcohol or nicotine consumption by the mother, and more specifically relates to a composition comprising vitamin C for preventing or treating nerve cell damage in fetuses in mothers that have been exposed to alcohol or nicotine, and relates to a method for protecting nerve cells in fetuses by administering mothers with the composition.
US8257691 Composition and dosage form comprising a particle formulation and suspending vehicle A liquid composition in an osmotic drug delivery system and a dosage form in an osmotic drug delivery system is disclosed comprising an amphiphilic molecule, a non-aqueous liquid solvent, and a pharmaceutically active agent.
CA2371174C Cyclo-alkyl substituted benzimidazoles and their use as parp inhibitors The invention relates to a compound of formula (I) or (II), wherein A represents a saturated or mono-unsaturated carbocycle containing 3 to 8 carbon atoms which can also have a condensed benzol ring, whereby the rings can also be substituted with one or two different or identical radicals; R1 represents hydrogen, chlorine, fluorine, bromine, iodine, branched and unbranched C1-C6-alkyl, OH, nitro, CF3, CN, NR11R12, NH-CO-R13, O-C1-C4 alkyl; and R2 represents hydrogen, branched and unbranched C1-C6 alkyl, C1-C4 alkyl-phenyl. The invention also relates to the tautomeric forms, possible enantiomeric and diastereomeric forms, possible cis-trans isomers on the rings in Aand their prodrugs. The substituted benzimidazoles of general formulas (I) and (II) are inhibitors of poly(ADP-ribose) polymerase (PARP), or poly(ADP-ribose) synthase (PARS), as it is also known and can be used for the treatment or prophylaxis of diseases which are associated with the increased enzyme activity of this enzyme.
CA2234610C New amino acid derivatives, processes for preparing them and pharmaceutical compositions containing these compounds The invention relates to new amino acid derivatives of general formula I R1 - R11 - A1 - A2 - NR2R3 (I) and the pharmaceutically acceptable salts thereof, wherein R1, A1, A2 , R2, R3 and R11 have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin)-antagonists.
EP1267883B1 Bile secretion promoting composition for liver transplantation containing a 15-keto-prostaglandin Disclosed is a bile secretion promoting composition comprising a 15-keto-prostaglandin compound as an active ingredient. The composition is useful for treatment of a subject having a condition or disease associated with bile secretion deficiency and also for treatment of a liver to be transplanted in a liver transplantation process.
US20100104529 TNF-alpha VACCINE FOR TREATING DISEASE CONDITIONS MEDIATED BY PATHOLOGICAL TNF-alpha The present invention provide TNFα-defensin/chemokine fusion polypeptides and polynucleotides and methods of treating, inhibiting or preventing disease conditions mediated by pathological TNFα, including chronic neuropathic pain, chronic inflammation, insulin resistance, diabetes, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia and artherosclerosis, by administering a therapeutically effective amount of the TNFα-defensin/chemokine fusion polypeptides and polynucleotides.
EP2402357A1 Analogs of 2',3'-dideoxy-3'-fluorothymidine 5'-monophosphate (FLTMP) for treatment human immunodeficiency virus (HIV), their application and pharmaceutically acceptable form of drug Analogs of 3'-fluorothymidine 5'-monophosphate (FLTMP), preferably intended 2',3'-dideoxy-3'-fluoro-β-D-erythro-pentofuranoside of thymine 5'-monophosphate (FLTMP): 3'-fluoro-2-thiothymidine 5'-monophosphate intended 2',3'-dideoxy-3'-fluoro-β-D-erythro-pentofuranoside of 2-thiothymine 5'-monophosphate; 3'-fluoro-4-thiothymidine 5'-monophosphate is intended 2',3'-dideoxy-3'-fluoro-β-D-erythro-pentofuranoside of 4-thiothymine 5'-monophosphate (4-SFLTMP). This invention includes also medical use of analogues of 3'-fluorothymidine 5'-monophosphate (FLTMP), according to the invention, Formula 1, for therapy of infections caused by the human immunodeficiency virus (HIV-1) wild type strain and strains showing resistance and multidrug resistance. The inventors unexpectedly discovered that proposed new FLTMP analogs with thiosubstituent at 2 or 4 position of FLT pyrimidine ring and monophosphate group at 5'-0-of 2,3-dideoxyribose exert very potent inhibitory activity against drug and multidrug resistant HIV-1 strains, as well as show high selectivity and good solubility in water. This invention also includes pharmaceutical acceptable form of drug, which according to the invention, contain known acceptable media and auxiliary substances, containing, as an active compounds analogues of general Formula 1, in which X, Y and R have the above-mentioned importance, especially the relationship being dilithium salt of 2-SFLTMP and 4-SFLTMP.
EP2087888A1 Adenosine a1 receptor antagonists for the treatment of alkalosis The present invention relates to adenosine A1 receptor antagonists (AA1RA), for use in treating alkalosis.
WO2012134445A1 An improved process for the preparation of paliperidone The present invention relates to a process for preparation and purification of 3-[2-[4-(6- fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H- pyrido[1,2-a]pyrimidin-4-one, also known as paliperidone or 9-hydroxy risperidone.
CN103374015A Camptothecin derivative and preparation method thereof as well as application of camptothecin derivative in preparation of medicine for treating tumours The invention discloses a camptothecin derivative and a preparation method thereof as well as application of the camptothecin derivative in preparation of a medicine for treating tumours. The camptothecin derivative has the following structural general formula: the derivative, salt and composite thereof are used for preparing medicines for treating cell proliferation diseases and cancers of mammals. Through self medicine molecular design and further biological activity determination on the prepared and synthetized compound in vitro and in vivo, the camptothecin derivative is found to have obvious activity in inhibiting all cancers, and shows good effect in a model for inhibiting the growth of tomours of mice.
EP1121109B1 Biphasic tramadol preparation The invention relates to a pharmaceutical preparation, especially for oral administration, having at least one active substance and formulation components influencing the release of the active substance. Said preparation comprises at least one opioid analgesic as active substance, which is formulated proportionally for rapid and retarded release in such a way that the in vitro release rate from the preparation according to the Ph. Eur. Paddle Method showed a mean value of more than 40 % by weight after one hour, wherein the average value of the in vitro release rate after four hours was still less than 80 % by weight of the active substance.
CN103142478A Calcitriol emulsion and preparation method thereof The invention relates to a calcitriol emulsion and a preparation method thereof. The emulsion is prepared from the following ingredients in percentage by weight: 0.0005% of calcitriol, 0.7-1.2% of meglumine, 12-18% of polyethylene glycol 400, 1.5-2.5% of polyethylene glycol 6000, 0.5-30% of vegetable oil, 4.0% of emulsifying agent, 1.0% of coemulsifier and the balance of water for injection. According to the emulsion, the content of calcitriol is remarkably increased, so that the drug dosage is reduced; and the stability of calcitriol to light and air is improved, and the bioavailability of calcitriol is also remarkably improved.
WO2013187052A1 Anti-colon cancer agent The present invention addresses the problem of providing an effective anti-colon cancer agent. The present invention is characterized in that administering a substance that suppresses expression of FAM83H protein, such as siRNA, against FAM83H, which is a protein known to be involved in forming dental enamel, or administering a substance that blocks the function of FAM83H protein, such as anti-FAM83H protein antibodies, (1) suppresses proliferation of colon cancer cell lines, (2) induces apoptosis in colon cancer cell lines, and (3) suppresses the motor function of colon cancer cells. Using the present invention makes it possible to collect data for assessing anti-colon cancer agents or the risk of colon cancer occurrence/recurrence.
WO2007046087A3 Pharmaceutical compositions and diagnostic methods for inflammatory skin disesaes, disorders or conditions The invention relates to the treatment or prevention of an inflammatory skin disease, disorder or condition, by modulating a protein that is normally regulated by caspase-8 in the skin or by increasing caspase-8 activity or level in the skin. Another aspect of the invention relates to methods for diagnosing an inflammatory skin disease, disorder or condition or a predisposition to develop said disease disorder or condition in an individual. Further aspects of the invention relate to methods for identifying target proteins involved in the course or pathology of an inflammatory skin disease, disorder or condition and to methods of screening a candidate compound for treating said disease, disorder or condition. In particular, the invention relates to inflammatory skin diseases such as atopic dermatitis and psoriasis.
WO2006082820A1 Therapeutic agent for herpes progenitalis [PROBLEMS] To provide a therapeutic useful for the treatment of herpes progenitalis after the development of lesions. [MEANS FOR SOLVING PROBLEMS] An N-[2-[(4-substituted phenyl)amino]-2-oxoethyl]tetrahydro-2H-thiopyran-4- carboxamide derivative in which the phenyl group is substituted at position 4 by a 5- or 6-membered heteroaryl group has a good anti-herpesvirus effect and can exert good therapeutic effect on herpes progenitalis after the development of lesions. Therefore, this compound is useful for the treatment of herpes progenitalis after the development of lesions.
CN102670618A Application of spiclomazine and anti-pancreatic cancer pharmaceutical preparation The invention relates to the technical field of medicines and discloses application of spiclomazine in preparation of anti-pancreatic cancer medicines and anti-pancreatic cancer pharmaceutical preparation of the spiclomazine. Compared with clinical medicine gemcitabine, a compound in the application and the pharmaceutical preparation has significant effect on pancreatic cancer cell inhibition, has low toxicity for human normal cells, can inhibit intrusion and metastasis of pancreatic cancer cells, and can be well applied in curing of pancreatic cancer and the preparation of the anti-pancreatic cancer medicines.
EP2782643A1 Androgen receptor ligands Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (AR) is a member of the Nuclear Receptor (NR) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (DHT). Synthetic androgens and anti-androgens have therapeutic value in the treatment of various androgen dependent conditions, from regulation of male fertility to prostate cancer. Current treatment of prostate cancer (PCa) typically involves administration of 'classical' antiandrogens, competitive inhibitors of natural AR ligands, DHT and tes, for the ligand binding pocket (LBP) in the C-terminal ligand binding domain (LBD) of the AR. However, prolonged LBP-targeting can often lead to androgen resistance and alternative therapies and therapeutic strategies are urgently required. Disclosed herein are a class of non-steroidal, small molecule AR antagonists which inhibit the transcriptional activity of the AR by non LBP-mediated modulation. The novel class reported demonstrates full ('true') antagonism in AR with low micromolar potency, high selectivity over both the Estrogen Receptors alpha and beta (ERα and ERβ) and the Glucocorticoid Receptor (GR) and only micromolar partial antagonism in the Progesterone Receptor (PR). Data provide compelling evidence for such non-LBP intervention as an alternative approach to classical PCa therapy. (Formula I).
US20100129418 Method of inducing negative chemotaxis using an ellagitannin or gallotannin The current invention is directed to methods of inducing the negative chemotaxis of a migratory cell comprising contacting the cell with a compound selected from the group consisting of an ellagitannin and a gallotannin. In one embodiment, the compound is ellagic acid or a pharmaceutically acceptable salt thereof.
US20110112194 Medicaments Containing Pantothenic Acid This invention relates to medicaments and their use in the alleviation of inflammation and pain in joints.
WO2005092351A1 The medical use of graft nano-carbon The present invention relates to use of graft nano-carbon in the manufacture of medicaments for targeting lymph or killing the metastasis cancer cells in lymph nodes directly. The graft nano-carbon is the nano-carbon which is modified on the surface to graft hydrophilic group. The graft nano-carbon could disperse in the water and form suspension, without suspending agents and without the grind dispersing apparatus having the higher shearing force. The effect of graft nano-carbon on targeting lymph is better than that of nano-carbon suspension, the graft nano-carbon could kill the metastasis cancer cells in lymph nodes directly and could be used as chemical therapy medicaments. The increasing active group of surface could combine with chemical therapy medicaments in covalent bond, thus there maybe develop a graft nano-carbon chemical therapy medicaments for targeting lymph.
US20130281530 Methods of therapeutic monitoring of phenylacetic acid prodrugs The present disclosure provides methods for adjusting the dosage of PAA prodrugs (e.g., HPN-100, PBA) based on measurement of PAA and PAGN in plasma and calculating the PAA:PAGN ratio so as to determine whether PAA to PAGN conversion is saturated.
US7951395 Rapid release, water permeable self adhesive polymer matrix system; photodynamic therapy and/or diagnosis of skin lesions The invention relates to a dermal for aminolaevulinic acid, wherein a self-adhesive matrix system is used containing crystalline aminolaevulinic acids.
CN103655640A Biological active matter eye cleaning fluid The invention relates to biological active matter eye cleaning fluid which is mainly applied to treatment of dry eyes, sore eyes, blurry eyes and other symptoms of people wearing contact lenses and people facing a computer for long time, has the effects of moistening eyes and washing out contamination, and also can be used for preventing and reducing conjunctivitis and keratitis. The biological active matter eye cleaning fluid has the characteristics that (1) efficiently moisturizing and nourishing ingredients can be used for relieving sore eyes, hyperaemia, blurry eyes and other symptoms; (2) biological degerming ingredients can be used for effectively removing bacteria entering the eyes as well as preventing keratitis, conjunctivitis and pinkeye; (3) irritating ingredients are excluded, so that damages to the eyes and hypersensitivity can be avoided; (4) dirt in eyes can be effectively removed, and the eyes can be bright; (5) the cleaning liquid can be used as the cleaning liquid of contact lenses.
CN102048919A Externally-applied drug for treating and preventing hair loss The invention discloses a formula of an externally-applied drug for treating and preventing hair loss. The externally-applied drug is characterized by being prepared from alum, pepper seeds, pinellia ternate and the like, and the formula is as follows: 20 to 30 g of alum, 20 to 40 g of pepper seeds, 10 to 15 g of pinellia ternate, 5 to 10 g table salts, 50 to 70 ml of vinegar and 1000 to 2000 ml of water. The externally-applied drug disclosed by the invention is healthy and easy to use, and is an ideal externally-applied drug for treating hair loss.
US7396848 oxazole derivatives to treat diabetic neuropathy and/or other kinds of peripheral neuropathy; 4-(4-chlorophenyl)-5-[3-(2-methoxyphenoxy)propyl]-2-(2-methyl-1-imidazolyl)oxazole A neurotrophin production/secretion promoting agent which comprises an azole derivative of the formula: wherein R1 represents a halogen atom, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, a thiol group which may optionally be substituted, or an amino group which may optionally be substituted; A represents an acyl group which may optionally be substituted, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, or a carboxyl group which may optionally be esterified or amidated; B represents an aromatic group which may optionally be substituted; X represents oxygen atom, sulfur atom, or nitrogen atom which may optionally be substituted; and Y represents a divalent hydrocarbon group or heterocyclic group, or a salt thereof; which is useful as an agent for preventing or treating neuropathy.
US7300922 Enhancing or inhibiting the biological activity of nucleic acid ligands by administrating a modulator, to change the binding of the nucleic acid ligand for its target or degrading or cleaving The biological activity of nucleic acid ligand is regulated (i.e. enhanced or inhibited) in vivo to produce a desired biological effect. This is accomplished through the administration of a modulator, or regulator, that changes the binding of the nucleic acid ligand for its target or that degrades or otherwise cleaves, metabolizes or breaks down the nucleic acid ligand while the ligand is still exerting its effect. Modulators of the present invention can be administered in real time as needed based on various factors, including the progress of the patient, as well as the physician's discretion in how to achieve optimal therapy. Thus, this invention provides for the first time a regulatable therapeutic regime in the course of nucleic acid ligand therapy.
CN1966050A Medicament for treating heart disease and preparation process thereof Disclosed is a medicament for treating heart disease and its preparation, wherein the raw materials include liquidambar orientalis mill 0.3-2g, gum benzoin 0.3-2g, frankincense 3-12g, Loranthus mulberry mistletoe 10-18g, stem of mistletoe 10-30g, Ligusticum wallichii 3-15g, root of Chinese trichosannthes 10-15g, ginkgo leaves 5-12g, wild or spiny jujuba seed 1.5-5g, tuber fleeceflower stem 10-35g, red peony root 6-15g, root of red rooted saliva 3-12g, spicebush root 5-12g, giant knotweed rhizome 10-30g, wrinkled gianthyssop 5-10g, sandalwood 5-10g, borneol 0.03-0.1g, psoralea fruit 6-9g, cassia twig 3-12g, curcuma longa 3-10g, dalbergia wood 3-6g, prepared fleece-flower root 6-15g, astragalus root 10-20g, ilex pedunculosa 30-60g, prepared rhizome of rehmannia 15-30g, tetrandra root 5-12g, panicled swallowwort root 3-12g, notoginseng 3-12g, corydalis tuber 3-15g, curcuma root 5-15g, safflower 3-15g, achyranthes and cyathula root 6-30g, campanumaea pilosula 6-15g and dried wood-louse 10-30g.
WO2008018426A1 Pyrimidine derivative as pi3k inhibitor and use thereof Disclosed is a medical agent which is excellent in stability in living bodies and water solubility, while having excellent PI3K inhibitory activity. The medical agent is thus useful for prevention or treatment of cancers. Specifically disclosed is a compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. (I) (In the formula, X represents a single bond or the like; Y represents a single bond or the like (provided that X and Y are not single bonds at the same time); Z represents a hydrogen atom or the like; m represents an integer of 1 or 2; and R1 represents a cyclic substituent.)
CN101904913A Extravasated blood pain removing agent The invention discloses a method for preparing an extravasated blood pain removing agent. The method comprises the following steps of: cooling realgar, peach kernel, pseudo-ginseng, rheum officin and herba lycopi at a temperature of -20 DEG C for 36 hours, taking out and cooking in a casserole for 60 minutes with river water at 40 DEG C, cooling and then removing the impurities so as to obtain the agent, the method can remove the extravasated blood quickly.
US20110150941 Epithelial delivery The present invention relates to composition comprising vesicles and associated with the vesicles, a chemical agent, for use in a method of treatment by therapy wherein the chemical agent is delivered trans- and/or intra-epithelially to a human or animal body, wherein the constructs comprise an amphiphilic block copolymer having a hydrophilic and a hydrophobic block. Methods for forming the composition are also provided.
WO2011008675A2 Catecholamine compounds, compositions, and formulations, and methods of using the same The invention relates to catecholamine compounds, compositions, and formulations comprising those compounds, and methods of treating Parkinson's disease with those compounds, compositions, and/or formulations.
CN102512688A Nilestriol-beta-cyclodextrin inclusion compound and preparation method thereof The invention discloses a nilestriol-beta-cyclodextrin inclusion compound and a preparation method thereof. The nilestriol-beta-cyclodextrin inclusion compound is prepared from nilestriol and beta-cyclodextrin at a mole ratio of 1 to 1. Drug auxiliary materials are added into the nilestriol-beta-cyclodextrin inclusion compound, so that the nilestriol-beta-cyclodextrin inclusion compound is prepared into an oral solid preparation through a proper preparation process. According to the preparation method disclosed by the invention, the solubility of the nilestriol in water is improved, and the nilestriol-beta-cyclodextrin inclusion compound is good for being absorbed and functioned.
EP1613307A2 M sb 3 /sb muscarinic acetylcholine receptor antagonists Novel thiazole aniline compounds, pharmaceutical compositions, methods of making them and used therof in treating M3 muscarinic acetylcholine receptor mediated diseases are disclosed
WO2010006261A1 Methods for inducing stem cell migration and specialization with ec-18 The present invention relates to promoting stem cell migration and specialization by administering one or more MADG compounds. The present invention further pertains to repairing or promoting the healing of injured tissue or a wound of an individual by administering a MADG compound (e.g., EC- 18) to the individual, or subjecting the injured tissue/wound to a MADG compound. Another aspect of the invention relates to treating disease or conditions that benefit from stem cell therapy by administering MADG with or without exogenous stem cells.
EP2402322A1 1,2,3,4-tetrahydroisoquinoline derivative and its use as orexin receptor antagonist The invention relates to the compound (R)-2-[(S)-1-(3,4-Dimethoxy-benzyl)-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-N-isopropyl-2-phenyl-acetamide; and to its use as active ingredient in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compound, pharmaceutical compositions containing the compound and methods of treatment comprising administration of said compound to a human being.
CN1951380A Medical usage of salvianolic acid B salt and total salvianolic acid The invention ligatures the single ureter into mouse kidney fiber mode, watches the stomach treatment function on DS. Wherein, the 3D mouse is randomly divided into four groups as false surgery group, mode group, DS group and anode contrast chlorine group; after 7 days after feeding drug, killing the mouse, taking out the kidney, slicing with paraffin, colorizing with HE, watching in light lens; the experiment proves that the DS group and anode contrast group have similar kidney state and mode; but the DS group and anode contrast chlorine group have reduced expansion degree of nephric tubule epithelial cell, to reduce the foam generation, and the ill parts are distributed in sheets, whose range is less than 25% and different significance is lower than 0.05; using 293 cell to detect the effect of DS on the fiber cell increment, while the result proves that when DS density is 500mg/ml, it can restrain the 293 cell increment caused by vessel contract element II, similarly as the restrain function of DS on the mouse kidney filter process.
US20100189789 Micronized Tanaproget, Compositions, and Methods of Preparing the Same The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, magnesium stearate, micronized edetate calcium disodium hydrous, and micronized sodium thiosulfate pentahydrate. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.
US20050191267 Mulberry extract; whitening effects for darkened skin through antityrosinase activity, antioxidant and anti-inflammatory properties A process is provided for obtaining Mulberry extract that is of higher quality than presently available commercial extracts. The extracts may be provided in cosmeceutical raw material forms, including a paste, liquid or powder that can be added to cosmetics to provide whitening effects for darkened skin through anti-tyrosinase activity, and antioxidant and anti-inflammatory properties.
US20090162289 A tetrapyrollic photosensitizer compound with one pendant CH2CH2CON(CH2CON(CH2COOH)2)2 or N(CH2COOH)2 group, being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide; water soluble photosensitizing and imaging compounds; hyperproliferative tissue A tetrapyrollic photosensitizer compound having at least one pendant —CH2CH2CON(CH2CON(CH2COOH)2)2 or —N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has the formula: or a pharmaceutically acceptable derivative thereof, wherein R1-R8 and R10 are various substituents and R9 is substituted or unsubstituted —CH2CH2CON(CH2CON(CH2COOH)2)2; or —N(CH2COOH)2. The invention also includes a method of treatment by photodynamic therapy by treatment with light after injecting the compound and a method of imaging by fluorescence after injection of the compound.
EP1931424A2 P13k inhibitors for the treatment of endometriosis This invention relates to a method of treating and/or preventing endometriosis comprising administering a P13K inhibitor. The P13K inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis-related infertility.
WO2010045601A3 Synergistic combination of sphingosine-1-phosphate receptor antagonists and antimicrotubule agents This invention is based on the discovery that the administration of a sphingosine-1- phosphate receptor antagonist (SlP) and at least one chemotherapeutic agent selected from the the group of antimicrotubule agents provides an unexpectedly superior treatment for cancer. Antimicrobial agents such as the taxane compounds are known in the art, for example, paclitaxel (available as TAXOL® from Bristol-Myers Squibb, Princeton, NJ.), docetaxel (available as TAXOTERE® from Sanofi-aventis, Bridgewater, NJ.) and the like and other compounds that act as antimicrotubule agents, such as Vincristine (ONCOVIN®, VINCASAR PFS®, VCR), Vinblastin (VELBAN®, VELSAR®) and Vinorelbine, and similar compounds. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one sphingosine-1 -phosphate 1 (SlPlR) receptor antagonists, and at least one antimicrotubule agent.
CN103356588A Application of Sarcaboside A in preparing medicine for treating or preventing renal fibrosis The invention discloses an application of Sarcaboside A in preparing a medicine for treating or preventing renal fibrosis, belonging to the technical field of a new application of a medicine. The application of the Sarcaboside A in preparing a medicine for treating or preventing renal fibrosis is disclosed for the first time; since a brand new skeleton type is adopted and the inhibitory activity on renal fibrosis is unexpectedly strong, the possibility of other compounds giving any prompt is avoided, and the Sarcaboside A has outstanding substantive features; and a remarkable progress is made in applying the Sarcaboside A to the prevention of renal fibrosis.
US7417050 Cognition activators; Alzheimer's disease; attention deficit disorders; Parkinson's disease; Huntington's disease; neurodegenerative disease Compounds of formula I: and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and the use of such compounds and compositions for use in therapy.
EP2158205B1 3,3-spiroindolinone derivatives as anticancer agents There are provided compounds of the general formulas (Ia), (Ib) 5 wherein X, Y, R1, R2, R3, R4 and R5 are as described herein. The compounds exhibit anticancer activity.
US20090247640 Antimicrobials having polyquaternary ammoniums and alcohol-bearing amidoamines and methods for their use Antimicrobial or preservative compositions with high user comfort and/or low ocular irritation. The compositions comprise a polyquaternary ammonium compound and an amidoamine having an alcohol group and exhibit synergistic antimicrobial activity. The compositions may be used as stand-alone antimicrobials/preservatives or may be incorporated into other ocular compositions such as those for ocular lens care or the treatment of ocular conditions.
US20110251566 Apparatuses, methods, and compositions for the treatment and prophylaxis of chronic wounds According to an illustrative embodiment a method to promote healing of a wound is provided comprising contacting the wound with a biologically active composition comprising a lipoic acid derivative and gelatin. In another embodiment a wound dressing is provided comprising a scaffold coated with a biologically active composition comprising a lipoic acid derivative. In a further embodiment, a system is provided for treating a tissue site of a patient, the system comprising a reduced-pressure source to supply reduced pressure, a manifold to distribute reduced pressure to a tissue site and a scaffold coated with a biologically active composition comprising a lipoic acid derivative. Methods for producing such a system and scaffold are also disclosed.
CN101766563A Combination use method of water-soluble vitamin injection and sodium chloride injection The invention discloses a combination use method of water-soluble vitamin injection and sodium chloride injection and relates to chemical medicine field. The invention aims to solve the problems in prior art that: the vitamin injection and sodium chloride injection are not suitable for diabetes patients, and are mixed to generate 5-hydroxymethylfurfural so that the toxic side reaction incidence is increased and the clinical use becomes inconvenient and the economical burden is heavy for patients. The technical scheme for solving the technical problems includes that: the combination use method of the water-soluble vitamin injection and sodium chloride injection is characterized in that a water-soluble vitamin injection is dissolved in 10-500 ml of 0.9% NaCl injection solution to be mixed uniformly, and then the mixed injection is used for Intravenous Infusion. The invention has the advantages that the combination use method of water-soluble vitamin injection and sodium chloride injection is suitable for diabetes patients, avoids generating 5-hydroxymethylfurfural, guarantees the medication safety and convenient clinical use and reduces the medical expense for patients.
US20110136850 Methods and compositions for topoisomerase i modulated tumor suppression Disclosed herein are methods and compositions for determining the sensitivity or enhancing the sensitivity of cells to the effects of topoisomerase I inhibitors. Also disclosed are methods and compositions for inducing cell death, apoptosis and/or growth arrest which may be used for tumor suppression.
WO2011036299A1 Irreversible inhibitors useful for the treatment of kinase-related pathologies The present invention provides new compounds (I) having a kinase inhibitory activity and useful for treating cancer.
EP2011504A1 Skin cream for treatment and/or cleaning of skin for neurodermitis Use of silver particles with an average particle size of 1-100 mu m for the treatment of neurodermitis, is claimed. An independent claim is included for a composition comprising silver particles and evening primrose oil. - ACTIVITY : Dermatological; Hypnotic; Antipruritic. - MECHANISM OF ACTION : None given.
CA2748963A1 Tetrahydronaphthalen-2-ol derivatives The present invention relates to novel tetrahydronaphthalen-2-ol derivatives, to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the manufacture of a medicament for the prevention or treatment of lower urinary tract symptoms,benign prostate hyperplasia,prostate cancer,hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer.
CN102526740A Novel high-efficiency antiemetic medicinal composition The invention relates to a novel high-efficiency antiemetic medicinal composition. The novel high-efficiency antiemetic medicinal composition is prepared by combining active ingredients comprising Aprepitant or Fosaprepitant and a 5-hydroxytryptamine 3 receptor antagonist with pharmaceutically auxiliary materials.
CN102060842A 3-(substituted xylylenimine-2-yl)-2,6-piperidine diketone polymorph and medical composition The invention discloses a polymorph of 3-(4-amino-1-oxo-1,3-dihydro-2H-isoindole-2-yl) piperidine-2,6-diketone. In addition, the invention discloses a preparation method and a medical composition of the polymorph.
WO2012020989A3 Pharmaceutical or cosmetic composition containing nicotinic acid adenine dinucleotide phosphate or derivative thereof The present invention relates to a use of nicotinic acid adenine dinucleotide phosphate or a derivative thereof for promoting the differentiation of keratinocytes into fibroblasts. The present invention provides a pharmaceutical or cosmetic use of a composition containing NAADP or a derivative thereof for regenerating and improving a skin barrier, or preventing, improving or treating stratum corneum disorders such as psoriasis or atopy, and a use for promoting the differentiation of separated keratinocytes.
CN1748684A Oxibendazole nasal jelly for treating allergic rhinitis The present invention relates to the preparation process of nasal oxibendazole jelly and the application of the nasal oxibendazole jelly in treating allergic rhinitis.
US20140235564 Methods for treating neural cell swelling A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.
WO2012167133A3 Inhibitors of anandamide transport and their therapeutic uses Nucleic acid and polypeptide sequences corresponding to FLAT, a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1), are provided. FLAT lacks amidase activity but binds the endocannibinoid anandamide and facilitates its transport into cells. A chemical scaffold for the inhibition of anandamide transport is identified. Compositions of the invention prevent anandamide internalization in vitro, interrupt anandamide deactivation in vivo, and cause profound CB1 cannabinoid receptor-mediated analgesia in a mouse model of inflammatory pain. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the modulation of anandamide transport would be of benefit.
EP1964837A1 Anti-tumor agent for multiple myeloma The object of the invention is to provide a pharmaceutical composition and a therapeutic method which can exert their effects with higher efficiency on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR3, a cell that has a t(4;14) translocation and a cell expressing mutant FGFR3. The compound represented by General Formula (I), a pharmacologically acceptable salt thereof or a solvate thereof can exert their effects with higher efficiency on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR3, a cell that has a t(4;14) translocation and a cell expressing mutant FGFR3.
CN101443324A Benzylamine derivatives as CETP inhibitors The present invention provides a compound of formula (I): said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
WO2012089220A1 Method for producing a water-soluble medicinal form of an antibiotic from the group consisting of rifamycins, and composition produced by said method The present invention relates to the field of medicine, pharmaceutics, nano-technology and colloidal chemistry, in particular to a method for producing a water-soluble medicinal form (pharmaceutical composition) of an antibiotic from the group consisting of rifamycins, such as rifabutin, rifampicin, rifapentin, rifaximin and the pharmaceutically acceptable derivatives thereof for the treatment of tuberculosis. The problem addressed by the claimed solution is to simplify the technology for producing a pharmaceutical composition of the antibiotic from the group consisting of rifamycins, and also to eliminate highly toxic chloroorganic solvents. The claimed technical solution is directed towards producing a pharmaceutical composition of the antibiotic from the group consisting of rifamycins suitable for parenteral (intravenous) administration to a patient requiring treatment. The above-mentioned composition is produced by a method comprising a) dissolving the antibiotic from the group consisting of rifamycins in an organic solvent selected from a group consisting of solvents which mix with water; b) adding an aqueous solution of albumin produced by dissolving albumin in a 1-10% molar ratio in sterilized demineralized water to the solution produced in step a); c) stirring the mixture produced; d) filtering said mixture; e) adding a cryoprotector; f) freezing said mixture; g) drying said mixture (lyophilically or by spray drying).
US20080032983 Ortho-Substituted N'-Benzylidene-(3-Hydroxyphenyl)Acethydrazides Novel ortho-substituted N′-benzylidene-(3-hydroxyphenyl)acetohydrazides of the formula (I), in which R1-R9 have the meanings indicated in Claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.
US20120141557 Highly-mineralized osteogenic sponge compositions and uses thereof Osteogenic sponge compositions having enhanced osteoinductive properties for use in bone repair are described. The compositions include a quickly resorbable porous carrier, a more slowly resorbed mineral scaffold and an osteogenic factor, preferably a bone morphogenetic protein. The compositions enable increased osteoinductive activity while retaining a reliable scaffold for the formation of new bone at an implant site. Methods for therapeutic use of the compositions are also described.
US20120082718 Morphine Formulations Described is a pellet composition comprising a core element comprising morphine sulfate, a filler and a binder, wherein the morphine sulfate, calculated as the anhydrous form, comprises about 50 wt % to about 85 wt % of the total weight of the core element; and a coating disposed on at least a portion of the core element, the coating comprising an insoluble matrix polymer which is insoluble at pH 1 to 7.5; an enteric polymer which is insoluble at pH 1 to 4 and soluble at pH 6 to 7.5; and an acid soluble polymer which is soluble at a pH of 1 to 4, wherein the ratio of the acid soluble polymer to the enteric polymer is 1.45:1 to 2.5:1 on a weight basis. Also described are dosage forms comprising the disclosed pellets.
EP1343771B1 3-ox(adi)azolylpropanohydroxamic acids useful as procollagen c-proteinase inhibitors Compound of formula (I), wherein X is C1-6 alkylene or C2-6 alkenylene, each of which is optionally substituted by one or more flluorine atoms; R is aryl or C3-8 cycloalkyl optionally substituted by one or more fluorine atoms; W is N or CZ; are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP.
WO2009136162A1 Intermediate and processes involved in the preparation of 2 ' -cyano-2 ' -de0xy-n4-palmit0yl-1-beta-arabin0furan0sylcytosine The present invention relates to a process for preparing a compound of formula (682-6'), said process comprising the steps of: formula (682-4), (682-5), (682-6'): (i) converting a compound of formula (682-4) into a compound of formula (682-5); and (ii) converting said compound of formula (682-5) into a compound of formula (682- 6'). Further aspects of the invention relate to the use of the above process in the preparation of 2'-cyano-2'-deoxy-N4-palmitoyl-l-β-D-arabinofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
CN103340924A Wind-dispelling and pain-relieving oil and preparation method thereof The invention relates to a wind-dispelling and pain-relieving oil and a preparation method thereof. The wind-dispelling and pain-relieving oil is composed by the following raw materials by weight: 90-110 parts of litsea cubeba oil, 20-40 parts of cinnamon oil, 1-3 parts of bee venom and 1-3 parts of borneol. The preparation method of the wind-dispelling and pain-relieving oil comprises the following steps of grinding bee venom and barneol into fine powder; mixing the litsea cubeba oil and the cinnamon oil; then adding the powder of bee venom and barneol into a mixture of the litsea cubeba oil and the cinnamon oil; stirring to make the raw materials solvated thoroughly; loading the mixture into a container; and sealing for over 40 days. The wind-dispelling and pain-relieving oil can be used for treating various diseases such as headache and arthralgia due to pathogenic wind-dampness; headache, stomachache and arthralgia caused by cold; sudden sprains and contusion, muscular pain and arthralgia caused by falls, abdominal distention and pain due to dyspepsia, etc.
EP1844044A1 Thiazole-4-carboxamide derivatives as mglur5 antagonists The present invention is concerned with novel thiazole 4-carboxyamide derivatives of the general formula (I) and with methods for the preparation thereof, which compounds are useful as metabotropic glutamate receptor antagonists: wherein R1 to R4 are as defined in the specification.
CN102671081A Medicine for treating pimples The invention discloses a medicine for treating pimples. The medicine is a medicine composition prepared from purely natural plants, animals and minerals according to a certain process. The medicine has a special curative effect on acne, not only is high in curative effect, but also avoid recurrence after a person is cured, the raw materials of the medicine are wide in source, cost is low, a preparation method is simple, and discharge of waste gas, waste water and industrial residues is prevented during production.
CN101032463A Sirolimus injection and preparing technique thereof The sirolimus injection is prepared through the following steps: dissolving sirolimus in pharmaceutically acceptable solvent, adding cosolvent and water for injection via stirring to dissolve, adding excipient via stirring to dissolve, filtering, ultrafiltering to obtain clarified solution without heat source, loading into antibiotic ampule, and freeze drying to obtain freeze dried sirolimus powder. Where, the solvent is ethanol, etc; the cosolvent is soluble polyvinylpyrrolidone, hydroxypropyl-beta-cyclodextrin and/or nicotinamide; the weight ratio between sirolimus and the cosolvent is 1 to 2-5; the excipient is mannitol, lactose, etc; and the weight ratio between sirolimus and the excipient is 1 to 0.5-5. The sirolimus injection of the present invention has stable quality, high bioavailability and high curative effect.
CN102229603A Triazole heterocycle-containing 2-methyl benzofuran compound, and preparation and application thereof The invention discloses a triazole heterocycle-containing 2-methyl benzofuran compound shown as a formula (I), and a preparation method and application thereof. In the formula (I), R1 is substituted phenyl; R2 and R4 are benzoyl or substituted benzoyl independently; and R3 is H, hydroxyl, halogen, nitryl or C1-C3 alkyl. The invention has the advantages that: (1) the invention provides a new inhibitor medicament capable of obviously inhibiting activity of monoamine oxidase and provides research basis for screening new medicaments for resisting depression, parkinsonism and the like; (2) automatic operation is easy to implement, the synthetic process is accelerated, efficiency is improved, and raw materials can be recycled; and (3) the synthetic process is convenient to operate and is easily applied to synthesizing new compounds for screening high-flux compounds.
CA2215605C Osmotically controlled fermentation process for the preparation of acarbose The invention relates to a novel fermentative process for the preparation of acarbose. By monitoring and controlling the osmolality in the fermentation solution, a substantial improvement in yield from the fermentation is achieved.
WO2009097709A1 Pyrazolopyrimidinone-containing phenyl guanidine derivatives, pharmaceutical compositions containing them, process for their preparation and their use The invention relates to the pharmaceutical technology field, especially relates to pyrazolopyrimidinone-containing phenyl guanidine derivatives represented by formula I, pharmaceutically acceptable salts or solvates thereof. The invention also relates to pharmaceutical compositions containing such compounds and the preparation of such compounds. The compounds have stronger inhibitory effect against phosphodiesterase V than sildenafil, and have higher selectivity than to phosphodiesterase VI which distributes in retina, thus can be used in the treatment for vascular disorders such as erectile dysfunction of male.
CN101015555A Inclusion compound of lornoxicam and hydroxypropyl-beta-cyclodextrin and its preparation method The invention discloses an inclusion compound of non-steroidal anti-inflammatory drugs of lornoxicam and hydroxypropyl-beta-cyclodextrin and its preparation method. The inclusion compound comprises a certain amount of 1-40% hydroxypropyl-beta-cyclodextrin. The inclusion compound is prepared by dissolving lornoxicam in solution containing hydroxypropyl-beta-cyclodextrin for inclusion. It has the advantages of good dissolution in water, convenient preparation, and good stability against light, heat and wet; and has broad market prospect.
US20100221351 Controlled Drug Delivery Using a Thermally Responsive Nanocapsule to Augment Cryoablation In accordance with certain embodiments of the present disclosure, A method for intracellular delivery of cytotoxin in combination with cyoablation is provided. The method includes encapsulation of one or more cytotoxins in a thermally responsive nanocapsule by decreasing the temperature of the nanocapsule to increase the permeability of the nanocapsule whereby the one or more cytotoxins are sucked into or diffuse into the nanocapsule. The temperature of the nanocapsule is increased and the nanocapsule is delivered into a cell. Cryoablation is performed in proximity to the cell resulting in the release of the one or more cytotoxins from the nanocapsule into the cell.
US7732146 Method for screening an agent that modulates activity of macrophage migration inhibitory factor Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.
WO2014158998A1 Substituted pyridine and pyrazine compounds as pde4 inhibitors The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non- human animal training protocols, and treating treating peripheral disorders, including inflammatory and renal disorders.
US7060836 Lactams as tachykinin antagonists Compounds of the formula (I): or a pharmaceutically acceptable salt, prodrug, solvate or polymorph thereof, wherein R, R1, and Z are as defined herein, are useful in treating or preventing a condition for which an NK2 antagonist is efficacious.
US20080254110 Composition For Enhancing Immunity and Reducing Inflammation Related to Infections A composition and method for enhancing immunity and reducing or inhibiting inflammation related innate immune system activation while affording the body of a user protection against known detrimental byproducts of immune-response is provided. The composition comprises at least a therapeutically effective amount of vitamin C and extract of Andrographis paniculata. The present invention may additionally comprise vitamin A (Retinyl palmitate), an extract of blackberry, garlic, and an extract of cranberry. A method of same is also provided.
US7338948 Use of quetiapine A method of treating Attention Deficit Hyperactivity Disorder, Conduct Disorder and related disorders which comprises using the atypical antipychotic agent quetiapine.
US20110319326 Derivatives of benzothiazines, preparation thereof and application thereof as drugs The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11β-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably R1 represents a hydrogen or OR1 represents an ester or an ether. R2 represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R3 represents a methyl or ethyl; R4 and R′4 represent a hydrogen.
CN1850041A Anticancer medicine slow-release preparation containing platinum compound and its synergist The present invention relates to an anticarcinogen slow-released injection containing platinum compound and its synergist. It is composed of microsphere and solvent, in which the microsphere includes anticancer effective component and slow-released auxiliary material, the solvent is general one or special solvent containing suspension adjuvant. The anticancer effective component includes platinum compound selected from heptylplatin, loplatin, neidaplatin, oxaliplatin, denaplatin or enloplatin and/or platinum compound synergist selected from antitumor antibiotic, antimetabolite medicine, taxane and/or plant alkaloid; the slow-released auxiliary material is selected from polylactic acid copolymer, ethylene-vinylacetate copolymer, difatty acid and sebacic acid polymer and poly (fumaric acid-sebacic acid) copolymer. The suspension adjuvant is selected from sodium cellulose glycollate, and its viscosity is 100 cp-3000 cp (20 deg.C-30 deg.C). The slow-released microsphere also can be made into slow-released implant preparation.
CN102335194A Compound preparation of montmorillonite The invention relates to a compound preparation of montmorillonite. The compound preparation is characterized by being prepared by adding a zinc salt into montmorillonite, wherein the weight ratio of the montmorillonite to the zinc salt is 1:(0.0016-0.044). The compound preparation is used for treating diarrhea, peptic ulcer and zinc deficiency, and has the advantages of no side effects, simple production process and good effects for treating diarrhea, peptic ulcer and zinc deficiency.
EP0949920B1 Highly selective butyrylcholinesterase inhibitors for the treatment and diagnosis of alzheimer's disease and dementias The present disclosure relates to the discovery that highly selective butyrylcholinesterase inhibitors can prevent or treat cognitive impairments associated with aging or Alzheimer's disease. A preferred butyrylcholinesterase inhibitor is cymserine.
CN101007008A Ciclesonide medicinal spraying agent and its preparation method The invention discloses a Ciclesonide medicinal water spray agant and its preparing process, wherein the constituents include (by weight portions): Ciclesonide 1 part, solvent 0.2-4 parts, emulsifying agent 0.04-4 parts, water 0.2-0.4 part. The process requires no casting agents such as CFC and HFC, thereby no pressure containers are needed.
US20100239655 Taurine-based compositions and therapeutic methods Taurine and derivatives thereof may be used in conjunction with agents that activate or up-regulate the Taurine Transporter so as to enhance hydration of the skin and repair the skin bather, prevent apoptosis and oxidative damage in the skin, and heal or prevent photo-induced skin damage. The presence of biogenic taurine or taurine derivatives in tissues and/or body fluids can be used as a biomarker for tissue trauma. Detection and/or quantification of such biogenic taurine or derivatives form the basis for an assay for determining the presence and/or extent of tissue damage.
CN101439040B Medical use of 2-O-alpha-L-rhamnose-4,6,4'-trihydroxybenzophenone The invention relates to the field of natural drugs as well as medicines and health protection, in particular to a usage of 2-O-Alpha-L-rhamnose-4, 6, 4'-trihydroxyl benzophenone in the aspects of medicines and health protection as well as cosmetics, i.e. the 2-O-Alpha-L-rhamnose-4,6,4'-trihydroxyl benzophenone can be used for preparing a drug for curing anaphylactic diseases and used for preparing pain relievers and antioxidant drugs.
US20120115923 Sirna Compositions Promoting Scar-Free Wound Healing of Skin and Methods for Wound Treatment This invention describes compositions and methods using siRNA to target various genes expressed in cells of injured tissue during scar formation to promote scar-free wound healing.
WO2011097546A2 Topical antibiotic formulations A biocompatible antibiotic formulation suitable for application to skin tissue, the formulation including: (a) a silver(II) oxide; (b) a hydrophilic clay; and (c) a base, said silver(II) oxide and said hydrophilic clay being intimately dispersed within a base.
CN101217966B Combination therapy of cancer with AZD2171 and gemcitabine The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with gemcitabine; to a pharmaceutical composition comprising AZD2171 and gemcitabine; to a combination product comprising AZD2171 and gemcitabine for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and gemcitabine; to the use of AZD2171 and gemcitabine in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeabilityreducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.
WO2012135561A1 Formulations comprising 2 -amino- 2- [2- (4 - octylphenyl) ethyl] propane -1, 3 - diol A solid pharmaceutical composition suitable for oral administration, comprising: (a) a S1P receptor modulator; (b) a filler, and (c) a cyclodextrin.
WO2010123769A1 Compositions and methods for treating ocular inflammation with lower risk of increased intraocular pressure A composition for treating or controlling an ocular disease or condition comprises a dissociated glucocorticoid receptor agonist ("DIGRA"), which disease or condition has an etiology, or results, in inflammation. The composition can optionally include an anti-inflammatory agent, an anti-infective agent, or both. The composition can be formulated for topical application, injection, or implantation in an affected eye to treat or control the ocular inflammatory disease or condition.
CN1562032A Gatifloxacin gels ear drops and its preparing method An auristillae o Jiatishaxing gel contains Jiatishaxing, carbomer and triethanolamine. Its preparing process is also disclosed.
US20120220543 Treatment of Glaucoma and Other Retinopathies with Gangliosides A method of treating or preventing a retinopathy such as glaucoma in a human patient in need thereof comprising administering one or more gangliosides to the patient.
WO2010064300A1 Composition for treatment of esophageal cancer Disclosed is a compound represented by the general formula (I) shown below, a salt of the compound, or a hydrate of the compound or the salt, which is useful in a composition for the treatment of esophageal cancer. [Formula] (I) wherein R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 independently represent a hydrogen atom; R4, R5, R6 and R7 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like; R8 represents a hydrogen atom or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; and X represents a group represented by the formula: -CH= or a nitrogen atom.
WO2012114252A1 Novel indole and pyrrolopyridine amides The present invention relates to indole and pyrrolopyridine amide derivatives of formula (I) wherein R1, R 2, R 3, U, V, W, X, Y, Z and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
US20100266716 Natural Photodynamic Agents and their use The present invention is safe photodynamic agents and their use in treating microbial contamination.
CN101723933A Piperidine-4-ketone-O-substituted oxime triadimenol-type antifungal compound and preparation method thereof The invention provides a piperidine-4-ketone-O-substituted oxime triadimenol-type compound, namely a 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazole-1-group)propyl)piperidine-4-ketone-O-substituted oxime-type compound, hydrochloride, nitrate, hydrobromide and methane sulfonate of the same and a preparation method thereof. The compound has strong antifungal effect on various superficial and deep fungi, has the advantages of high efficiency, low toxicity and wide antifungal spectrum compared with antifungal medicaments in the prior clinical application, and can be used to prepare novelantifungal medicaments.
US7115559 Administering factor XIII to patients afflicted with bleeding due to a coumarin anticoagulant-induced vitamin K deficiency Use of factor XIII for treating coumarin-induced hemorrhage or bleeding. The coumarin may be warfarin or dicoumarol. A patient having coumarin-induced bleeding is treated with factor XIII alone or in conjunction with vitamin K.
WO2009027482A3 Tsh receptor antagonizing tetrahydroquinoline compounds The present invention relates the use of a compound, a pharmaceutical composition, compounds and a kit for treating or preventing disorders in a mammal responsive to TSH receptor mediated pathways, including disorders such as hyperthyroidism, Graves' disease, Graves Ophthalmopathy, Graves' associated pretibial dermopathy, nodular goitre and thyroid cancer comprising administering to said mammal an effective amount of a tetrahydroquinoline compound of Formula (I) or an pharmaceutically acceptable salt thereof.
US20090076060 Deuterium-enriched temsirolimus The present application describes deuterium-enriched temsirolimus, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CA2599937A1 Pharmaceutical compositions for the treatment and/or prevention of anxiety disorders The invention relates to new pharmaceutical compositions for the treatment and/or prevention of anxiety disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment and/or prevention of anxiety disorders and methods for the preparation thereof.
US20120077800 Methods for Treating Antipsychotic-Induced Weight Gain The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
CN102558224A Phosphorus propofol sodium hydrate and preparation method and purpose thereof The invention provides a phosphorus propofol sodium hydrate, which is specially a complex hydrate salt. The phosphorus propofol sodium hydrate contains 5 to 9 crystal water, can be obtained in isopropanol-water-alcohol mixed solution, can be used for preparing anaesthetic and can serve as the anaesthetic in an operation.
WO2011034951A2 Assisted enzyme replacement therapy Reagents and methods useful for the synthesis of conjugates comprising guanidinylated cyclic acetals are provided. Also provided are methods for increasing the cellular uptake of various therapeutic compounds and treatment modalities using these conjugates.
US20080027116 Pharmaceutical Composition for Treating Spinocerebellar Ataxia This invention provide to a pharmaceutical composition for treating spinocerebellar ataxia (or atrophy, degeneration) or multiple system atrophy, or for improving ataxia or equilibrium disturbance comprising a compound of the formula (I): wherein R is methyl, cyano or carbamoyl, a pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.
CN102824338A Application of s-oleylpropanolamide in preparing medicine for reducing blood fat and preventing and treating non-alcoholic fatty liver The invention discloses application of s-oleylpropanolamide in preparing a medicine for reducing blood fat and preventing and treating non-alcoholic fatty liver, relating to s-oleylpropanolamide. The s-oleylpropanolamide is a natural PPAR(alpha) agonist. According to the pharmacological experiment research, s-oleylpropanolamide has obvious effects on reducing blood fat and preventing non-alcoholic fatty liver, and can be used for preventing and treating hyperlipidemia and non-alcoholic fatty liver caused by multiple factors.
US20090117176 Anticancer Treatments A method of treating the human body for cancer comprises administering an effective therapeutic amount of a Pegylated Liposomal form of the anthracycline Doxorubicin (“PLD”), in combination with an effective therapeutic amount of ET-743
US20100061978 Methods for detecting and treating cancer Methods and kits for detecting cancer and monitoring cancer progression are described. The method involves analyzing a sample containing nucleic acids or proteins from a patient for decreased expression of endoglycan and/or increased expression of podocalyxin.
US20110182980 Composition for suppressing expression of target gene An object of the present invention is to provide a composition for suppressing expression of a target gene, and the like. A composition comprising an RNA-encapsulated liposome, wherein the RNA contains a sequence consisting of 15 to 30 contiguous bases of a target gene mRNA (hereinafter, sequence X) and a base sequence (hereinafter, complementary sequence X′) complementary to the sequence X, 1 to 90% of all sugars binding to the bases of the sequence X and the complementary sequence X′ being ribose substituted by a modifying group at 2′ position, and the lipid particle being capable of reaching a tissue or an organ containing an expression site of the target gene is provide.
CN1579380A Decanoy-acetaldehyde sodium frozen-dry powder injecta and preparation method The invention is a houttuynine sodium bisulfite freeze-dry powder injection solution and its manufacturing method. The character lies in: it uses houttuynine sodium bisulfite with effective dose as the effective ingredients, and it includes bracket solution, solubilizer and oxidization resisting agent. The manufacturing process is: a. the solubilizer is diluted with injection water according to the proportion in prescription, stirs, adds in houttuynine sodium bisulfite, blends with warm water to dissolve them; b. the bracket agent and the oxidization agent are put into the injection water, stirs them until they are dissolved, adds active carbon and boils them for 15 minutes, decarbonizes it with filter film; and adds then into the dissolved liquid in step a, adds in injection water and regulates the pH value between 3.0 and 4.5, the injection water is added to the whole quantity, carries on filter with micro-aperture filter film, samples, content measurement, backup; the product can be produced with current freeze-dry method. The merits of the invention are: quick absorption, quick effect, accurate dose and stable quality.
CN101843886A Medicine containing saussurea and for curing rheumatic bone disease and preparation method thereof The invention discloses a medicine containing saussurea and for curing a rheumatic bone disease and a preparation method thereof; the medicine is a preparation prepared from the following raw materials and components in parts by weight: 1 to 9 parts of saussurea, 0.5 to 1.5 parts of processed semen strychni, 0.1 to 0.9 parts of myrrh, 1 to 5 parts of safflower, 0.7 to 1.5 parts of heracleum hemsleyanum michaux, 1 to 2 parts of aconiti preparata, 1 to 3 parts of angelica dahurica, 0.5 to 1.5 parts of turmeric, and 0.1 to 0.5 parts of borneol. When in preparation, all the raw materials are crushed and then mixed uniformly; and the raw materials are further prepared into the required patches, papua, oral liquid, granules or capsules. The product has the effect of removing stasis and relieving pain, removing blood stasis and stimulating menstrual flow, activating blood and diminishing inflammation, dispersing pathogenic wind and removing dampness, sweating and relieving exterior syndrome, and warming and stimulating channels and collaterals, is used for curing pain and other symptoms caused by rheumatoid arthritis, rheumatoid cold joint pain, osteoarthritis, acute soft tissue injuries, joint sprains and chronic soft tissue damage, and also has a certain curative effect to cholecystitis, stomach pain, dysmenorrheal and other symptoms.
WO2004055026A8 Tetracyclic 3-substituted indoles having serotonin receptor affinity The present invention relates to novel substituted tetracyclic 3-substituted indoles, represented by general formula (I), its stereoisomers, its radioisotopes, its N-oxides, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates, its useful bio-active metabolites and any suitable combination of the above as well as processes for preparing such compounds of the general formula (I), its stereoisomers, its radioisotopes, its N-oxides, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates, its useful bio-active metabolites and also includes any suitable combination of the above.
EP2632460A2 Compositions and methods for treating tuberculosis The invention provides for the use of antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit anti-mycobacteria activity, including the mycobacterium causing tuberculosis. Multiple compounds were synthesized and screened for anti-tuberculosis activity. Disclosed herein are a series of compounds with anti-tuberculosis activity, including six leads that completely inhibited bacterial growth at 5 micrograms per ml or less. Three of these compounds were tested to determine MIC and these ranged between 1 and 4 micrograms per ml against both drug susceptible Mycobacterium tuberculosis strains and strains that are multi-drug resistant (MDR) including XDR strains. The compounds developed are derived from parent compound nitazoxanide, which had no inhibitory activity in the stringent testing format used herein. The derivatives were synthesized using a di-nitro-thiophene or 4-Chloro-5-Nitro-thiazole scaffold and R groups connected via a peptide bond (NHCO) to cyclic compounds such as benzene, thiophene or furans. Many of these compounds have broad spectrum activity against Gram positive bacteria including Staphylococcus aureus (MRSA) and Staphylococcus epidermidis. Several of these lead compounds were not toxic for mice at 200 mg/Kg doses administered over a period of three days.
US20110152321 Bicyclic derivatives useful as inhibitors of dpp-1 The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
CN103393066A High-potency sweetener composition with vitamin and compositions sweetened therewith Provided are high-potency sweetener composition with vitamin and compositions sweetened therewith. The present invention relates generally to functional sweetener compositions comprising non-caloric or low-caloric natural and/or synthetic, high-potency sweeteners and methods for making and using them. In particular, the present invention relates to different functional sweetener compositions comprising at least one non-caloric or low-caloric natural and/or synthetic, high-potency sweetener, at least one sweet taste improving composition, and at least one functional ingredient, such as a vitamin. The present invention also relates to functional sweetener compositions and methods that can improve the tastes of non-caloric or low-caloric high-potency sweeteners by imparting a more sugar-like taste or characteristic. In particular, the functional sweetener compositions and methods provide a more sugar-like temporal profile, including sweetness onset and sweetness linger, and/or a more sugar-like flavor profile.
US6916796 Producing a blunted glycemic response in a diabetic patient by administering pullulan The present invention is directed to the use of pullulan as a slowly digested carbohydrate and to its incorporation into food products, especially beverages and meal replacement products.
US20060069098 Bone disorders; reduce concentration of parathyroid hormone in blood A novel compound represented by the following formula (1) or a salt thereof: wherein symbol “A” represents a saturated heterocyclic group, a 5-membered heteroaromatic group having two heteroatoms in the ring, a group represented by the formula A1 (R2, R3, and R4 represent hydrogen atom, hydroxyl group, etc.), etc., B represents a group represented by the formula B1 (R11 represents hydrogen atom, hydroxyl group, etc.), etc., R1 represents an alkyl group, and symbol “n” represents an integer of 2 to 6, which has a parathyroid hormone depressing action and showing low toxicity, and a medicament containing the compound or salt thereof as an active ingredient.
WO2010086613A1 Compounds useful as inhibitors as ampk According to the invention there is provided a compound of formula (I), wherein, X, T, Y1 E, M, A1 to A5 and D1 to D5 have meanings given in the description, which compounds are useful in the treatment of cancer.
EP2490678A1 Coated capsules and tablets of a fatty acid oil mixture Compositions comprising a fatty acid oil mixture and at least one free fatty acid in a coated capsule or a coated tablet form suitable for oral administration, and methods of use thereof, are disclosed. Further disclosed are preconcentrates comprising a fatty acid oil mixture, at least one surfactant, and optionally at least one free fatty acid, in a coated capsule or a coated tablet form, and methods of use thereof. The preconcentrates are capable of forming a self-nanoemulsifying drug delivery system (SNEDDS), a self-microemulsifying drug delivery system (SMEDDS), or self-emulsifying drug delivery systems (SEDDS) in an aqueous solution.
US20090170888 Antipruritic Agent for Pruritus Caused by Multiple Sclerosis An antipruritic against pruritus caused by multiple sclerosis is disclosed. The antipruritic comprises as an effective ingredient an κ opioid receptor agonist compound having a 4,5-epoxymorphinan skeleton and having a specific chemical structure, such as Compound 1 having the following structure:
CN103550779A Application of ethylene diamine tetraacetic acid disodium in veterinary drugs The invention relates to application of ethylene diamine tetraacetic acid disodium in veterinary drugs. Ethylene diamine tetraacetic acid disodium can be used as a protective agent of drinking water type veterinary drugs, can prevent the drinking water type veterinary drugs from precipitating in water, and guarantees that the drug is absorbed by animal bodies in primary form, thus improving the absorptivity of drugs indirectly, and fully playing the effect of the drugs.
CN102210652A Lipid microsphere injection of larotaxel phospholipid compound, and preparation method thereof The invention relates to a lipid microsphere injection of a larotaxel phospholipid compound, and a preparation method thereof. The injection is composed of the larotaxel phospholipid compound, oil for injection, an emulsifier, a stabilizer, an antioxidant, an isotonic regulator and water for injection, wherein the larotaxel phospholipid compound is composed of larotaxel and phospholipid for injection; and the components of the injection in percentage by weight are as follows: 0.001-1% of larotaxel, 1-7% of phospholipid for injection, 5-25% of oil for injection, 0.2-0.8% of emulsifier, 0.02-0.2% of stabilizer, 0.01-0.5% of antioxidant, 1.5-3.5% of isotonic regulator and the balance of water for injection. The larotaxel lipid microsphere injection provided by the invention adopts the phospholipid compound as a drug-carrying means, thus obviously improving the drug-carrying amount; and 90% of the drug is enveloped in the oil phase and the oil-water interfacial film of the lipid microspheres, thereby improving the solubility and stability of the drug in the preparation, reducing the venous irritation and toxicity of the drug, and enhancing the anti-tumor curative effect of the drug. The preparation is used as an anti-tumor preparation and administered by venoclysis, and has low irritation, low toxicity, high efficiency and a targeting property.
CN102617435A Leucosceptrum canum chinone, preparation method and application The invention discloses a novel natural haematochrome, namely leucosceptrum canum chinone, a preparation and synthesis method thereof, as well as the application in the fields of foods and medicine. The leucosceptrum canum chinone is structurally a compound of parabenzoquinone and proline, and is the novel natural haematochrome. The leucosceptrum canum chinone provided by the invention is directly separated from nectar of leucosceptrum canum and is purified before being obtained; and meanwhile, the leucosceptrum canum chinone is obtained by adopting the simple and convenient synthetic method.The natural haematochrome of leucosceptrum canum chinone is nontoxic and safe, has high color gradation, is excellent in color protecting effect, is a new broom in edible pigments, can strongly restrain activity of receptor tyrosine kinase, and can be widely applied to the fields of foods and medicines.
WO2013190320A1 Imidazopyridines as inhibitors of aurora kinase and/or flt3 The present invention relates to compounds of formula I: wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The compounds of formula I are inhibitors of aurora kinase and/or FLT3. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which aurora kinase and/or FLT3 activity is implicated.
WO2012175654A1 Tetraline sulfonamide derivatives for use in the treatment of proliferative disorders Tetraline sulfonamides derivatives highly specific towards CA IX and/or CA XII human carbonic anhydrase for targeting solid tumors.
WO2014015047A1 Compositions and methods to treat neurodegenerative diseases The specification provides compositions and methods to treat neurodegenerative diseases.
WO2014023385A1 Pyridopyrimidine derivatives as protein kinase inhibitors Compounds of the formula (I) in which R, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and / or systemic lupus
US7632836 2-Morpholinoethyl ester of pivagabine; improved pharmacokinetic and therapeutic profiles; bioavailability; dosage; brain disorders; behavioral disorders; antidepressants; anxiolytic agents; neurodegenerative disorders; analgesics; eating disorders; antiarthritic agents; bipolar disorders; dysthymia The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine.
CN102448455A Use of flavonoids to increase the bioavailability of hesperetin The present invention relates generally to the field of hesperetin bioavailability. One embodiment of the present invention is directed at a composition that allows to increase the bioavailability of hesperetin and consequently to maximize the beneficial health effects of hesperetin.
US20080242727 enhancing protein synthesis and decrease protein catabolism; combating muscle wasting associated with dieting and/or disease A composition that may include branched chain amino acids, alpha amino n-Butyrate and/or alpha amino-n-valerate works synergistically to enhance lean body mass and prevent body mass breakdown. The composition may also be coupled with other agents to a) provide an increased level of amino acids and/or protein in the body's total pool or b) increase markers for protein translation or decrease markers of protein turnover. The composition may be administered in a variety of ways including capsules, tablets, powdered beverages, bars, gels or drinks. Increasing lean body mass is import to athletes looking to enhance performance, in the event of certain muscle wasting diseases, and to the general population that loses muscle mass as it ages.
CN102887859A Compound having analgesic and anti-inflammatory activity, preparation method thereof and application thereof The invention discloses a compound with a general formula I, a preparation method thereof and an application thereof as an analgesic and an anti-inflammatory agent. In the general formula I, when the R1 is benzyl, the general formula I represents a compound 5a-s; and when the R1 is hydrogen, the general formula I represents a compound 6a-s. Analgesic activity of the compound provided by the invention is evaluated by using a mouse tail-flick model, and the anti-inflammatory activity of the compound is evaluated by using a xylene postauricular proinflammatory model. The experimental results show that the compound or the pharmaceutically acceptable salt thereof have excellent analgesic and anti-inflammatory activity, and can be used in the production of preparing analgesic and anti-inflammatory drugs.
CN102188457A Scientific treatment method for cancer and broad-spectrum medicament for curing cancer A scientific treatment method for cancer and a broad-spectrum medicament for curing cancer. The invention relates to a formation mechanism of cancer (malignant tumor), a scientific treatment method, and a formula and a preparation technology of a specific broad-spectrum medicament for curing cancer. Adopting a stereo strangling method, targeting medicament for treating cancer strangles cancer cells comprehensively from aspects of preventing mitosis of the cancer cells, blocking out DNA replication, inhibiting generation of new blood vessels, attacking the cancer cell membranes, cutting out energy supply and directly killing the cancer cells. According to clinic tests, the medicament with a strong lethality against cancer cells can disintegrate, liquefy, shrink and dispel tumors, and remove the cancer cells. The medicament is characterized by broad-spectrum cure for cancer, a rapid effectiveness, a high cure rate and low side effects, and has substantial effects of mitigating patient pain, raising survival quality and prolonging patient life, besides patients with curing conditions can be cured. Therefore, successful development of the medicament will substantially advance the process of human conquering cancer.
CN102973570A Cefpiramide sodium for injection The invention provides a preparation method of novel cefpiramide sodium for injection. The method is characterized in that sterile cefpiramide sodium raw materials are directly sub-packed in penicillin bottles in an environment with relative humidity of lower than 50% and at least hundred-level cleanliness, and no accessory is used in the sub-packing process. According to the method provided by the invention, the technological steps are simple and stable, no accessory is used, and the obtained product of cefpiramide sodium for injection has the characteristics of stable quality and quick dissolution; and moreover, the production efficiency is obviously improved, and the production cost is reduced.
US20110165199 Composition and Process for Bone Growth and Repair A composition for the induction of bone growth is disclosed. The composition includes a substrate, bone growth protein, and sources of calcium and phosphate. The composition is acidic which promotes high activity of the bone growth protein. The calcium and phosphate sources can be provided as an acidic calcium phosphate salt. Also disclosed are methods of the making the composition and methods of using it.
CN103450168A Acylhydrazone derivatives containing 1,3,4-oxadiazole and pyridine, and preparation method and use thereof Acylhydrazone derivatives containing 1,3,4-oxadiazole and pyridine have a structure represented by a general formula shown in the specification. In the formula, R is one of groups shown in the specification. The acylhydrazone derivatives containing 1,3,4-oxadiazole and pyridine have an obvious inhibition effect on bacteria, so the cylhydrazone derivatives containing 1,3,4-oxadiazole and pyridine can be used for preparing antibiotic medicines. The invention discloses preparation methods of the derivatives.
CN1771974A Application of hedgedog fungus mycelium oligose in preparing medicine The application of hedgedog fungus mycelium oligose in preparing medicine relates to the use of hedgedog fungus mycelium oligose. The hedgedog fungus mycelium fermenting extractum is processed through dilution with water and via stirring, centrifuging, adding alcohol to the centrifuged liquid, centrifuging to collect precipitate, adding distilled water to compound solution, dialysis of the solution to collect dialyzed outer liquid, concentration to obtain the hedgedog fungus mycelium oligose. The present invention has determined effective parts, clear structure, small dosage and obvious curative effect on acute and chronic gastritis, gastric ulcer and chronic atrophic gastritis.
US6916477 Vaccine containing attenuated virus; induction antibodies; veterinary medicine The present invention is directed to a method of producing attenuated forms of bovine viral diarrhea (BVD) virus by mutating the Npro protease gene. The invention includes the attenuated viruses made by this method, antibodies generated using these viruses, and vaccines that can be used for immunizing cattle.
WO2006121557A1 Pregabalin free of lactam and a process for preparation thereof The present invention encompasses Pregabalin substantially free of Lactam and a process for obtaining Pregabalin substantially free of Lactam comprising extracting an acidic mixture containing a complex of Pregabalin with a strong mineral acid, with a C3-8 alcohol; and combining the organic phase with an organic base.
CN101735218A Piperidine carbamic acid ester derivative and application thereof The invention provides a piperidine carbamic acid ester compound shown as the general formula I and possible isomers, medicinal salts, crystal forms, hydrates, solvates and medical compositions thereof. The invention also relates to applications of the possible isomers, the medicinal salts, the crystal forms, the hydrates, the solvates and the medical compositions in preparing medicaments for treating and/or preventing diseases related to DPP-IV, such as diabetes mellitus, particularly for non-insulin-dependent diabetes mellitus and impaired glucose tolerance, and the applications have good property of in vivo pharmacokinetics.
CN101791297A Atorvastatin calcium oral disintegrating tablet and preparation method thereof The invention provides an atorvastatin calcium oral disintegrating tablet prescription and a preparation method thereof. The atorvastatin calcium oral disintegrating tablet prescription comprises atorvastatin calcium, a bitter covering agent, a filling agent, a disintegrant, a lubricant, and the like. The invention is technically characterized by providing a particle preparing technology which not only can effectively cover the bitter of the atorvastatin calcium, but also can lead the atorvastatin calcium oral disintegrating tablet to be disintegrated in the mouth. The atorvastatin calcium oral disintegrating tablet with pressure of above 4kg and disintegrating time within 30 seconds can be prepared by adding normal supplementary materials of filling agents, disintegrants, lubricants, and the like of oral disintegrating tablets and is easy to realize industrial scale production.
WO2008076417A1 (1r,6s)-2-azabicyclo[4.3.0] nonane-8,8-diphosphonic acid and its use in treating or preventing bone disorders, for example, osteoporosis or paget's disease Disclosed is a new composition of matter, substantially enantiomerically pure (1R,6S)-2-Azabicyclo-[4.3.0]nonane-8,8-diphosphonic acid, methods of preparing this new composition of matter, a pharmaceutical composition comprising the new composition, and administration of the composition in methods of treating bone disorders such as osteoporosis, osteolytic bone metastasis, rheumatoid arthritis and osteoarthritis.
EP2049092A2 Compositions with enhanced elasticizing activity Compositions for improving the elasticity of the vagina and of the perineum during the last trimester of pregnancy, include combining a thiolated compound or mixture thereof with an ester of organic acid or mixture thereof . The compositions according to the present invention improve the elastic properties of the vaginal and/or perineal tissues in terms both of increased extensibility and faster elastic recovery. The compositions according to the present invention may decrease risk of trauma of perineal tissues during delivery, as well as risk of rectal or bladder incontinence as a post-partum short/medium/long term complication.
WO2009077844A3 Inhibitors of biofilm formation of gram-positive and gram-negative bacteria The present invention relates to the use of compounds as broad spectrum inhibitors of bacterial biofilm formation. In particular the invention refers to a family of compounds that block the quorum sensing system of Gram-negative and Gram-positive bacteria, a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of bacterial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.
CN103239722A Regulating effect of 5-HT2C receptor-specific agonist on basic rhythmical respiration discharge of mammal medulla oblongata The invention discloses a novel use of a 5-HT2C receptor-specific agonist, namely regulating effect of the 5-HT2C receptor-specific agonist on basic rhythmical respiration discharge of mammal medulla oblongata. The invention provides an application of the 5-HT2C receptor-specific agonist in preparing a product, and the functions of the product are as indicated in (a) and/or (b) and/or (c): (a) prolonging the inspiratory time of basic rhythmical respiration discharge of a hypoglossal nerve root; (b) shortening the respiratory cycle of basic rhythmical respiration discharge of the hypoglossal nerve root; and (c) increasing the discharge integral amplitude of basic rhythmical respiration discharge of the hypoglossal nerve root. The 5-HT2C receptor-specific agonist can be specifically MK212. The invention discovers and functionally proves that adjustment of basic rhythmical respiration discharge participated in by the 5-HT2C receptor exists on a newborn rat in vitro medulla oblongata slice.
EP1289573B1 A medicinal aerosol antidiabetics formulation This invention relates to a medicinal aerosol formulation and more particularly, to a medicinal aerosol formulation containing a beta -cell hypoglycemic agent and a fluid carrier.
CN101810620B Methionine-vitamin B1 composite injection and preparation method thereof The present invention relates to the medical field, in particular to a methionine-vitamin B1 composite injection and a preparation method thereof. The composite of the invention comprises the following components in parts by weight: 10 parts of methionine, 1 part of vitamin B1, 10-50 parts of sorbitol and 0.001-0.01 part of sodium pyrosulfite. The composite injection of the invention has the advantages of high stability and the like.
CN103393946A Drug for treating type-2 diabetes The invention provides a drug for treating type-2 diabetes. The drug comprises, by weight, 3-8 parts of gypsum, 4-10 parts of balsam pear, 6-12 parts of Chinese yam, 10-15 parts of root of kudzu vine, 8-12 parts of radix astragali, 6-18 parts of mulberry, 8-16 parts of polygonatum rhizome, 4-12 parts of Chinese magnoliavine, 15-25 parts of bletilla striata and 10-15 parts of wolfberry. The drug has the advantages of good treatment effects and small side effects.
CN102973945A Trypsin-regulated nanometer supramolecular vesicles and preparation method and application thereof The invention discloses trypsin-regulated nanometer supramolecular vesicles. According to a building unit, a sulfonated cup [4] aromatic hydrocarbon serves as a host, protamine serves as a guest, and a supramolecular assembling body is built through host-guest inclusion complexation interaction. The preparation method comprises the following steps of: dissolving the sulfonated cup [4] aromatic hydrocarbon and the protamine in water, and uniformly mixing to obtain a target of a supramolecular vesicle solution; and adding trypsin into the target, so that supramolecular vesicles in the supramolecular vesicle solution are completely depolymerized. The method has the advantages that the preparation method of the nanometer supramolecular vesicles is easy and convenient, and raw materials of the host and the guest are less; the nanometer supramolecular vesicles have high biocompatibility and stability and have high response selectivity on the trypsin; and moreover, the supramolecular vesicles can be loaded with hydrophilic broad spectrum anti-cancer medicinal molecule adriamycin, and the loaded adriamycin can be released to a targeting locus of the trypsin with high selectivity and has wide application prospect in the fields of targeting drug delivery and treatment of pancreatic cancer.
CN101836974A Rivastigmine-hydrogentartrate-containing pharmaceutical composition and preparation method The invention discloses a pharmaceutical composition containing an active ingredient rivastigmine hydrogentartrate. The pharmaceutical composition comprises the rivastigmine hydrogentartrate and microcrystalline cellulose with weight percent of more than 50 percent, and then other excipients are added to be made into a corresponding formulation. The invention effectively solves the problem of hygroscopicity.
EP1025124B1 Low-toxicity human interferon-alpha analogues The present invention describes a method of reducing the cytotoxicity of interferon-alpha by making defined amino acid substitutions in the N-terminal portion of the polypeptide sequence. Also described are human interferon-alpha analogs with low cytotoxicity, and therapeutic applications of the low-toxicity interferon-alpha analogs.
EP1274464B1 Compositions and methods for regulated protein expression in gut The invention provides compositions and methods useful for treating disorders treatable by producing a protein in a regulatable manner in a mucosal cell or tissue of an animal. The treatment methods include in vivo and ex vivo methods, including transplanting in vitro transformed cells that secrete the protein into a mammalian subject.
WO2010007074A1 Pyrazolo [1, 5-a] pyrimidine derivatives The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
WO2007132138A1 Pharmaceutically acceptable salts and polymorphic forms The present invention is concerned with new risedronate salts and new polymorphic forms thereof, specifically a pharmaceutically acceptable tetra-(alkali metal) salt of risedronic acid and new polymorphic forms thereof, processes of preparing the same, pharmaceutical compositions containing the same, therapeutic uses thereof and methods of treatment employing the same.
CN101918392A Pyrazole derivatives as 5-LO inhibitors The invention relates to compounds of formula (I) processes for their preparation, their use as 5-lipoxygenase inhibitors and pharmaceutical compositions containing the same.
CN103655561A Pharmaceutical composition containing losartan potassium and amlodipine besylate and preparation method thereof The invention belongs to the field of medical technology and discloses a pharmaceutical composition containing losartan potassium and amlodipine besylate and a preparation method thereof. The pharmaceutical composition is composed of the following components in parts by weight: 50 parts of losartan potassium, 5 parts of amlodipine besylate (based on the weight of amlodipine), 150-250 parts of microcrystalline cellulose, 20-40 parts of polyvinylpolypyrrolidone, 1-5 parts of fumed silica, 1-5 parts of magnesium stearate and 8-16 parts of OPADYR II; the pharmaceutical composition is prepared from powder by a direct tabletting process. The pharmaceutical composition disclosed by the invention is stable in property, simple in production process and capable of being quickly dissolved under a low pH condition.
CA2233315C Pharmaceutical compositions containing hydroximic acid derivatives The invention refers to pharmaceutical compositions suitable for the protection of a mitochondrial genome and/or a mitochondrion from damages or for the treatment of diseases connected with such damages, said compositions comprising a hydroximic acid derivative of formula (I) or a pharmaceutically acceptable acid addition salt thereof.
CN101879165A Novel antihypertensive medicament compound preparation The invention discloses an antihypertensive medicament compound preparation. The compound preparation comprises a mixture of 20 to 400 weight parts of piperazine ferulate and 5 to 100 weight parts of losartan potassium which are used as medicinal compositions. The invention provides a kind of an angiotensin II receptor blocker (ARB) in a piperazine ferulate and RAS inhibitor, namely alosartan potassium compound antihypertensive preparation, which has the advantages of convenient administration and safe using. The antihypertensive medicament compound preparation focuses on carrying out omnidirectional control on the systolic pressure so as to certainly reduce the diastolic pressure, can not only remove vasoconstrictor effect of ET, but also remove vasoconstrictor effect of Ang II and also removes the pathologic vascular proliferation effect of the ET and the Ang II. Aiming at the conventional main known pathologic neurohumor factors causing hypertension, the novel antihypertensive medicament compound preparation has effect of reducing the systolic pressure furthest and simultaneously brings the effect of reducing the diastolic pressure.
WO2012112862A3 Treating mycobacterial infection with cu+/++ boosting therapeutics Provided herein are methods of treating a subject with a mycobacterial infection. The methods comprise administering to the subject a Cu+/++ boosting therapeutic. Also provided are compositions comprising a Cu+/++ boosting therapeutic. Further provided are methods of screening for a Cu+/++ boosting therapeutic.
CN101774921A Method for preparing dicaffeoylquinic acid methyl compound and composition thereof The invention relates to a method for preparing a dicaffeoylquinic acid methyl compound and an anti-influenza and antihepatitic medicine composition thereof. The method for preparing a dicaffeoylquinic acid methyl compound has the following steps of: extracting from woodbine, separating and modifying to obtain the dicaffeoylquinic acid methyl compound; and preparing the anti-influenza and antihepatitic medicine composition thereof. A great amount of anti-influenza and antihepatitic medicine composition containing dicaffeoylquinic acid methyl compound used as effective ingredients can be produced from plants with low dicaffeoylquinic acid methyl compound content by the invention.
CN102488706A Medicament for preventing and treating urinary calculus and preparation method and application thereof The invention provides a medicament for preventing and treating urinary calculus. The medicament consists of the following substances in parts by weight: 2-5 parts of citrate, 1-2 parts of nano-selenium, 2-4 parts of taurine and 1-3 parts of algal polysaccharides. The invention further provides gel of the medicament. The gel is prepared by cross linking 2-5 parts of citrate, 1-2 parts of nano-selenium, 2-4 parts of taurine, 1-3 parts of algal polysaccharides and 1-3 parts of chitosan. The invention further provides a preparation method of the gel and applications of the medicament and gel. The medicament has the advantages that: each component in the medicament supplement each other, coact, can be specific to a plurality of pathogens, and is remarkably superior to a single active ingredient of equal dose on the prevention and treatment of urinary calculus; the gel of the medicament has high permeability, the effect for preventing and treating urinary calculus is equivalent to that of oral administration, and the pain of operation or oral administration can be avoided for a patient; and each component of the medicament has plenty of materials and low price, so that the medicament is suitable for popularizing and applying.
WO2005027913A1 Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and a growth hormone secretagogue The present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof a combination of a 2-alkylidene-19-nor-vitamin D derivative and a growth hormone secretagogue or a pharmaceutically acceptable salt or prodrug thereof. Particularly, the present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D3 and a growth hormone secretagogue or a pharmaceutically acceptable salt or prodrug thereof. I
US20080035141 Aerosolized therapy kit A comprehensive aerosol therapy for administration to a patient in need of treatment is provided. More particularly, the aerosol therapy kit provides a seamless conduit for a patient to receive in-office or hospital inhalation treatments and access to drugs and equipment for continuing home use.
WO2009081219A1 Quinazoline derivatives as vanilloid receptor modulators There are provided quinazoline derivatives of the compounds of the formula (I): which may be used as vanilloid receptor modulators. Various related methods, formulations, variants, and embodiments are provided.
US20110301697 Manufacture, method and use of drug-eluting medical devices for permanently keeping blood vessels open The invention relates to stents and catheter balloons having optimized coatings for eluting rapamycin as well as methods for manufacturing these coatings.
DE102007035323A1 New diazen-1-ium-1,2-diolate substituted ketoconazole derivatives are ergosterol biosynthesis inhibitors useful as an active agent against microbial pathogenic germs, e.g. fungus, and an antiinflammatory active agent Diazen-1-ium-1,2-diolate substituted ketoconazole derivatives (I), are new. Diazen-1-ium-1,2-diolate substituted ketoconazole derivatives of formula (I), are new. Either R 1>, R 2>alkyl, arylalkyl, aminoalkyl, alkylaminoalkyl or a part of a polymer; or R 1>R 2>a hydrocarbon cycle with a ring size of 3-10 atoms containing one or more heteroatoms of O, S or N; and Z : methylene or alkylene. An independent claim is included for the preparation of (I). [Image] - ACTIVITY : Antibacterial; Fungicide; Antiparasitic; Antiinflammatory. - MECHANISM OF ACTION : Ergosterol biosynthesis inhibitor.
US20120041052 Compositions and Methods to Treat Muscular & Cardiovascular Disorders The present invention relates to a novel microRNA, mir-208-2, implicated in muscular and cardiovascular disorders. The present invention also relates to oligonucleotide therapeutic agents (antisense oligonucleotides and/or double stranded oligonucleotides such as dsRNA) and their use in the treatment of muscular and cardiovascular disorders resulting from dysregulation of mir-208-2.
CN102363008A Yin-toxin source eliminating pills The invention discloses Yin-toxin source eliminating pills which are a new effectual medicine which can treat dampness-heat and stasis diseases such as heat stranguria, stranguria due to chyluria, stranguria caused by overstrain, morbid leucorrhea, condyloma, herpes and the like. After research of years and clinical practice verification, the pills consist of rhizoma dioscoreae septemlobae, glabrous greenbrier rhizome, dandelion, philippine violet herb, sinkiang arnebia root, portulaca oleracea, coix seed, raw talc, amber, gardenia, phellodendron, dianthus superbus, polygonum aviculare, notoginseng root, medicinal cyathula root, costustoot, astragalus, red paeony root, barbed skullcap herb, raw rehmannia glutinosa, atractylodes lancea, bighead atractylodes rhizome, juncus effuses, cardamom, and liquorice tips; the pills are refined by the modern pill preparation method and have the effects of removing toxin and diminishing inflammation, clearing away heat and toxic materials, promoting the circulation of qi, and removing dampness through diuresis, treating stranguria and relieving pain and the like, can treat the diseases dampness-heat and stasis diseases such as heat stranguria, stranguria due to chyluria, stranguria caused by overstrain, and morbid leucorrhea, have a good curative effect, and quick response, are convenient to take and safe and reliable and can achieve the effects of addressing both the symptoms and root causes and fulfill the aim that the dampness-heat and stasis diseases hardly relapse after being treated; and the effective rate can reach 92 percent.
US20120183495 Avian colony stimulating factor 1 receptor binding proteins The present invention provides avian CSF1 genes encoding proteins which bind avian colony stimulating factor 1 receptor (CSF1R) and which exhibit immunomodulatory properties.
CN1600370A New chemical medicine in small molecule in use for curing dysmenorrhea and ache of bad rheumatoid arthritis A micro-molecular chemical emdicine for treating menalgia and serious rheumatic arthrodynia contains the nno-steroid inflammation-relieving analgesic, relative antidepresant and the active component for preventing gastric trouble and diarrhea.
CN103626738A Pomalidomide crystal and preparation method thereof The invention relates to the field of pharmaceutical chemistry, and discloses a novel pomalidomide crystal and a preparation method thereof. The novel pomalidomide crystal disclosed by the invention has the advantages of good crystal stability, high bioavailability, excellent property in the aspects of oral absorption and enhancement of immune response mediated by a T cell and a natural killer cell, weak toxicity and good storage and treatment stability and can be used for preparing pharmaceutical for treating multiple myeloma.
CN201658746U Moxibustion patch for insomnia A moxibustion patch for insomnia relates to the medical field and consists of a heater (1) and a nonwoven medicine pack (2), wherein the nonwoven medicine pack (2) is disposed on one face of the heater (1), and a plurality of pores are arranged on the other face of the heater (1). When in use, the nonwoven medicine pack (2) is fixed onto one face of the heater (1), the pores are arranged on the other face of the heater by a needle or a toothpick, then the patch can be attached to a specific acupoint, and the heater can constantly heat up for six to ten hours. The moxibustion patch has the functions of soothing nerves and brain, keeping calm, conditioning nerves and restoring normal sleep rhythm, the used medicines are non-toxic and have no side effects, and the patch reduces direct stimulation to digestive tracts and load to liver and kidney by means of gradual skin absorption, quickly improves sleep headache, amnesia and palpitation and dysphoria while guaranteeing no harm, is convenient in use, and is safe and reliable.
WO2010067131A1 P38 map kinase inhibitors The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
US8008321 Imidazo[1,5-a]pyridin-3-yl)(3-methoxy-4-nitrophenyl)methanone; a and b fibroblast growth factor receptors (FGFR) antagonist; anticarcinogenic, antitumor: lung, breast, prostate, melanomas, gliomas; antiinflammatory, vascular smooth muscle cells: atherosclerosis, restenosis, stent and bypass complications The invention concerns compounds of formula I, a method for preparing said compounds, pharmaceutical compositions containing same and the therapeutic uses thereof.
US20100028406 Topical drug delivery by iontophoresis The invention generally concerns methods of topical drag delivery. Delivery according to the invention may be via electrotransport of compounds through the skin, for example by iontophoresis. In certain embodiments improved methods for the delivery of compounds, such as antimicrobial agents are described.
EP1806364A2 New anti-IGF-IR antibodies and their applications An isolated antibody (Ab), and its functional fragments, that bind to human insulin-like growth factor-1 receptor (IGF-1R) and optionally: (i) inhibit natural binding of insulin-like growth factors (IGF)-1 and/or -2; and/or (ii) inhibit specifically tyrosine kinase activity of IGF-1R. An isolated antibody (Ab), and its functional fragments, that bind to human insulin-like growth factor-1 receptor (IGF-1R) and optionally inhibit natural binding of insulin-like growth factors (IGF)-1 and/or -2 and/or inhibit specifically tyrosine kinase activity of IGF-1R, is new. Ab comprises: (a) a light chain containing at least one complementarity-determining region (CDR) of one of 3 fully defined sequences comprising 16, 7 or 9 amino acids as given in the specification; or (b) a heavy chain containing at least one of the CDRs of one of 3 fully defined sequences comprising 6, 16 or 8 amino acids as given in the specification or sequences with 80% identity after optimal alignment. Independent claims are also included for the following: (1) murine hybridomas that secrete Ab; (2) an isolated nucleic acid (I) that: (a) is RNA or DNA and encodes Ab or its fragments; (b) is the complement of (a); or (c) has at least 18 nucleotides that can hybridize under stringent conditions with any of six sequences fully defined in the specification that encode the specified CDR, or with sequences having 80% identity after optimal alignment; (3) a vector containing (I); (4) a host cell containing the vector of (3); (5) a non-human transgenic animal containing at least one cell transfected with the vector of (3); (6) producing Ab or its fragments; (7) in vitro diagnosis of diseases induced by over- or under-expression of IGF-1R and or EGFR (epidermal growth factor receptor) by reaction with optionally labeled Ab; and (8) kit for performing method (7). - ACTIVITY : Cytostatic; Antipsoriatic. The murine antibody 7C10, specific for IGF-1R, was tested (at 250 Microgram twice a week, intraperitoneally) against MCF-7 breast cancer cells, implanted in nude mice. After 37 days, the mean tumor volume was about 150 mm3>; compared to about 800 mm3> for controls and 300 mm3> for animals treated with 10 Microgram tamoxifen. - MECHANISM OF ACTION : Inhibition of signal transduction pathways mediated by IGF-1R, optionally also by epidermal growth factor (EGF) receptor, thus inhibiting growth and/or proliferation of tumor cells, especially where dependent on IGF, EGF, estrogens and/or HER2/neu.
US20080280987 Methods of inhibiting angiogenesis and treating angiogenesis-associated diseases The invention provides methods of inhibiting angiogenesis in an individual by administering a composition (such as protein containing composition) comprising colchicine or thiocolchicine dimer. The composition is in an amount that is effective in inhibiting angiogenesis but is in some embodiments insufficient to induce significant cytotoxicity in the individual. The methods described herein are useful for treating angiogenesis-associated diseases, such as age-related macular degeneration, diabetic retinopathy, rheumatic arthritis, psoriasis, and cancer.
CN102432602A Mangiferin hepta-propyl-esterified derivative The invention discloses a method for chemically synthesizing a mangiferin hepta-propyl-esterified derivative and a pharmacological effect of resisting inflammation and reducing blood sugar of the derivative. The chemical structural formula of the derivative is shown in the specifications. The derivative has a remarkable effect of inhibiting mouse auricle tumefaction caused by dimethylbenzene; and the derivative has a remarkable effect of treating diabetic mice induced by alloxan.
CN101390832A Anti-cancer slow-release formulation loaded with carmustine and fluorouracil Disclosed is an anticancer sustainable-release agent, which contains the combination of carmustine and carmustine synergist which is selected from 5-FU, cisplatin or 06-benzylguanine. The anticancer sustainable-release agent is injection and implantation agent; the sustainable-release injection contains sustainable-release microspheres which contain effective anticancer ingredients and sustainable-release auxiliary material, and special solvent which contains suspending agent; the viscosity of injection is 50cp-1000cp(20 DEG C-30 DEG C); the suspending agent is selected from one or the combination of the followings, sodium carboxymethyl cellulose, mannitol, sorbitol, tween 80. The sustained-release auxiliary material is selected from copolymer of the combination of the followings, polylactic acid, ethylene vinyl acetate copolymer, polifeprosan, FAD: sebacic acid copolymer, polyglycolic acid and glycolic acid; the sustained-release auxiliary material is high-molecular polymer with biological capability and degradable absorption; the effective anticancer ingredients can be sustainably released on the local part of tumor during the degradable absorption process of the sustained-release auxiliary material so that the systemic toxic reaction caused by the sustained-release agent is obviously reduced; meanwhile, the effective medicine concentration is maintained in local part of the tumor.
CN102933205A Cilostazol cocrystals and compositions The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of cilostazol. Disclosed herein are several new compositions and cocrystals of cilostazol, including: a 1:1 cilostazol gentisic acid cocrystal, a 1:1:1 cilostazol gentisic acid H20 cocrystal, a 1:1 cilostazol 4- hydroxybenzoic acid cocrystal, and a 1:1 cilostazol 2,4-dihydroxybenzoic acid cocrystal. The therapeutic methods and uses of these cilostazol cocrystals are described as well as therapeutic compositions containing them.
US20130045993 Inhibitors of cyclin-dependent kinases and their use The present invention relates to novel compounds for the inhibition of cyclindependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R1, R2, R3, R4, R5, R6, R7, and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclindependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ia) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ia) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.
CN101474148B Oral liquid sustained-release preparation containing codeine and chlorphenamine and preparation method thereof The invention discloses an oral liquid sustained-release preparation containing codein and chlorphenamine and a preparation method thereof, aiming at solving the technical problem of realizing sustained-release micro-capsules coating of subparticle with the particle size being less than 100 microns. The oral liquid sustained-release preparation comprises the ingredients based on the following proportion by weight: 0.1-1.0% of codein, 0.01-1.0% of chlorphenamine, 0.1-10.0% of ion exchange resin, 0.5-30.0% of suspending aid, 0.001-5.0% of sustained-release material, 0.1-5% of acidity regulators, 0.01-5% of heavy metal ion complexing agent and the rest of water. The preparation method comprises: compound codein, chlorphenamine resin particles and medium are stirred to be prepared. Compared with the prior art, the invention adopts a surface-modified method to combine the sustained-release material with ion exchange property radical and empty radical which is obtained after the medicine isabsorbed by the ion exchange resin, a layer of compact sustained-release film is formed at the outer layer of medicine resin to control the releasing action of the medicine, thus realizing the sustained-release micro-capsule coating of subparticle with the particle size being less than 100 microns.
CN103202933A External application medicine composition used for treating fracture, and preparation method thereof The invention discloses an external application medicine composition used for treating fractures, and a preparation method thereof. According to the invention, musk, dragon's blood, and the like are adopted as raw materials. With the medicine provided by the invention, on a basis of high-efficiency swelling subsiding, pain relieving, blood circulation activating, stasis removing, tendon strengthening, and bone healing effects, both symptoms and root causes are treated.
WO2013045495A1 PYRANO[3,2-c][2]BENZOPYRAN-6(2H)-ONE DERIVATIVES AND USES THEREOF The present invention relates to new pyrano[3,2-c][2]benzopyran-6(2H)-one derivatives that act as SGLT2 inhibitors, which makes them promising candidates for the treatment of diabetes and other diseases and conditions mediated by SGLT2. These new drugs also exhibit platelet aggregation inhibitory activity which makes them promising candidates in the treatment and/or prevention of prothrombotic conditions. The invention also relates to the use of such pyrano[3,2-c][2]benzopyran-6(2W)-one derivatives in the treatment or prevention of the diabetes and other disorders and conditions mediated by SGLT2, as a single active ingredient or in combination with another antidiabetic agent or a drug for the treatment of hypertension, chronic heart failure or atherosclerosis, and pharmaceutical compositions comprising said new pyrano[3,2-c][2]benzopyran-6(2H)-one derivatives.
EP2140871A1 Suspension for visualization of transparent tissue in eye Disclosed is an ocular transparent tissue-visualizing suspension which can be used as an easy-to-handle and sufficiently safe means to enhance visibility of transparent tissues of the eye during a surgical operation on them. The ocular transparent tissue-visualizing suspension comprises, in an aqueous medium, fine particles of a biodegradable macromolecular compound and at least one salt selected from the groups consisting of salts of trivalent metals and salts of divalent metals.
CN103372182A Automatic vibration electromagnetic wave massage plaster and preparation method thereof The invention discloses an automatic vibration electromagnetic wave massage plaster and a preparation method thereof. The vibration electromagnetic wave massage plaster comprises an automatic vibration electromagnetic wave generator and a plaster attached on the automatic vibration electromagnetic wave generator, wherein the plaster comprises a plaster matrix and a plaster preparation coated on the plaster matrix; the plaster preparation is prepared from a resisting medium, raw salted aconite root, cortex cinnamomi, pepper and ginger powder, radix angelicae, pepper, sodium cyanide, asarum musk or menthol and borneol. The preparation method of the plaster comprises the following steps of: preparing raw materials in proportion, crushing, mixing, hot melting, coating on the plaster matrix, evenly thinning and molding, and coating on the automatic vibration electromagnetic wave generator to obtain the plaster. The plaster is available in raw materials, simple to prepare, low in cost, quick to take effect, high in curative effect and free of side effects.
CN103190611A Chrysanthemum capsules with blood sugar reducing function and preparation method thereof The invention discloses chrysanthemum capsules with a blood sugar reducing function, comprising the following components in percentage by weight: 15-40 % of chromium-rich chrysanthemum powder, 15-35 % of astragalus extract, 15-25 % of green tea extract, 10-21 % of American ginseng extract, 10-15 % of rhizoma anemarrhenae extract, and 5-10 % of licorice powder. The invention also discloses a preparation method for the health-care food, comprising the following steps of: weighing each raw material according to the weight percentage of the formula, sieving the raw materials respectively, and mixing for 20 to 30 minutes; taking magnesium stearate and starch or dextrin of which the total quantity is equal to the total mass of the raw materials as accessories, and sieving the accessories respectively; and mixing the sieved raw materials and accessories for 30 to 40 minutes, granulating, and filling granules into capsules. The chrysanthemum capsules are reasonable in formula, definite in health-care function, mild and safe, and do not have toxic or side effect; and by using the raw materials together, the health-care function of reducing blood sugar is realized.
EP1068182B1 Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one A process for preparing a compound of formula (1) in which P?1 and P2¿ are protecting groups; comprising a) reaction of a compound of formula (5) wherein P1 is as defined for formula (1); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P1 is as defined for formula (1); b) protecting the amino group to produce a compound of formula (7) wherein P?1 and P2¿ are as defined for formula (1); and c) selective reduction of the double bond to produce the compound of formula (1).
WO2009001126A1 Substituted piperidine derivatives and their use as antibaterial agents The present invention relates to compounds of Formula (I):and pharmaceutically acceptable salts thereof, and to their use in the treatment of bacterial infections.
US20120034316 Pharmaceutical compositions for dehydrating, atrophying and eliminating pathological tissues The present invention provides a pharmaceutical composition for dehydrating, atrophying and eliminating pathological tissues comprising inorganic polymeric ferric salt and/or inorganic polymeric ferric salt composite as its active ingredients, in which the inorganic polymeric ferric salt is polyferric sulfate, and the inorganic polymeric ferric salt composite is selected from a group consisting of poly-silicate ferric salts, polyphosphate ferric salts and their analogue. A surprising medical effect can be reached by treating pathological tissues with the pharmaceutical composition of the present invention which will make the treated pathological tissues dehydrated, atrophied, and absorbed or sloughed off. The pharmaceutical composition of the present invention is cost-effective, convenient to use and has significant effects in treatment of hemorrhoids, hemangiomas, varix, hygromas, abscess, tumors, scalding and burning wounds, bleeding traumatic wounds, and/or local injuries caused by chemical agents or microorganism.
US20120034297 Pharmaceutical dosage forms comprising 6'-fluoro-(N-methyl- or N,N-dimethyl-)-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1'-pyrano[3,4,b]indol]-4-amine A pharmaceutical dosage form for administration twice daily, once daily or less frequently, which contains 6′-fluoro-(N-methyl- or N,N-dimethyl)-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano[3,4,b]indol]-4-amine or a physiologically acceptable salt thereof.
EP2721033A1 Compounds, their pharmaceutical compositions and their uses as idh1 mutants inhibitors for treating cancers Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses as IDH1 mutants inhibitors for treating cancers are also provided.
CN101966201A Compound norfloxacin nicotinic soluble powder and preparation method thereof The invention discloses compound norfloxacin nicotinic soluble powder and a preparation method thereof, and provides soluble powder capable of treating poultry gastrointestinal infection and lowering drug resistance probability and the preparation method thereof. The compound norfloxacin nicotinic soluble powder is prepared from the following raw materials in percentage by weight: 3-10% of norfloxacin nicotinate, 5-15% of neomycin sulfate, 5% of sodium chloride, 5% of potassium chloride and the balance anhydrous glucose. In the invention, the norfloxacin nicotinate and the neomycin sulfate are taken as antibacterial ingredients, thus achieving double efficacies and effectively reducing the probability of bacterial drug resistance, wherein, the norfloxacin nicotinate can be absorbed into the bloodstream for killing pathogenic bacteria through circulation secretion, and the neomycin sulfate is rarely absorbed by oral administration and directly applied to intestinal tract for producing contact sterilization effect, so the norfloxacin nicotinate and the neomycin sulfate have good effect of killing the pathogenic bacteria resulting in the poultry gastrointestinal infection from the two aspects; and the combination of the sodium chloride and the potassium chloride can make up electrolyte loss caused by excessive diarrhea of infected poultry. Therefore, the combination of the drugs can strengthen the curative effect on the poultry bacterial gastrointestinal infection.
WO2013192506A1 Method and composition for alleviating tumor symptoms This invention relates to methods and compositions for treating carcinoid syndrome and other adverse symptoms associated with tumor-producing neuroendocrine tumors, said methods comprising administering a therapeutically effective amount of a vascular disrupting agent, or a pharmaceutically acceptable salt thereof, to a subject having a hormone producing neuroendocrine tumor. In preferred implementations, the vascular disrupting agent is combretastatin A-4 phosphate, combretastatin A-1 diphosphate, or a pharmaceutical acceptable salt thereof.
US20060287377 Vanilloid receptor 1 (VR 1) antagonists; efficacy; N-(3-Fluoro-4-methoxy-phenyl)-2-(7-nitro-1H-benzimidazol-1-yl)-acetamide, Compounds of formula I, wherein R1, m, R2, R3, p, n, R5 and R9 are as defined as in the specification, salts, solvates or solvated salts thereof, processes for their preparation, intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.
WO2007049586A1 Therapeutic agent for ulcerative colitis and/or crohn's disease Disclosed is a prophylactic or therapeutic agent for ulcerative colitis, Crohn's disease and/or Behcet's disease. The therapeutic agent comprises a highly unsaturated fatty acid derivative represented by the formula (1) as an active ingredient.
US20050175555 2,4,6,8,10,12,14-hexadecaheptaenol in cyclodextrins; antitumor , antiinflammatory, antiaging, antiprolifrative agent, antioxident; activation of free radical production, cardiovascular disorders, atherosclerosis; cosmetic and pharmaceutical use The invention relates to polyunsaturated linear aldehydes and derivatives thereof which can be extracted from the feathers or tissues of parrots of prepared synthetically with antioxidant, antitumoral and anti-inflammatory activity, and which are useful in the prevention and treatment of cardiovascular, inflammatory, atherosclerotic, proliferative cell and tumour damage and the prevention of alterations caused by ageing.
US20080306078 3,9-Diazabicyclo [3.3.1] Nonane Derivatives and Their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors This invention relates to novel 3,9-diazabicyclo[3.3.1]nonane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
US20090111839 Process for Preparing Amorphous Rosuvastatin Calcium of Impurities A pure amorphous form of rosuvastatin calcium substantially free from alkali metal impurities is disclosed. A process of preparing a pure amorphous form of rosuvastatin calcium is disclosed, which comprises hydrolysis of C1-C5 alkyl esters of rosuvastatin, preferably tert-butyl ester of rosuvastatin, with an organic nitrogen base, e.g. guanidines, amidines, amines and quaternary ammonium hydroxides, in the presence of water, optionally containing aprotic solvent, following the conversion of thus obtained rosuvastatin salt with a source of calcium to obtain rosuvastatin calcium, which is then isolated. An alternative process is disclosed, which comprises the conversion of numerous novel ammonium salts of rosuvastatin, preferably tert-octylammonium salt of rosuvastatin, with the source of calcium to desired commercial rosuvastatin calcium. Rosuvastatin calcium is an inhibitor of HMG CoA reductase, useful in the treatment of hyperlipidemia, hypercholesterolemia and atherosclerosis.
CN101239989A Nucleotide analog The invention relates to compounds or pharmaceutically acceptable salts, tautomers or solvates in a below formula (1a), wherein definition of each substituent is shown as claims, and the invention also relates to a preparation method thereof, and uses of the compounds in preparing medicines for curing the virus infection.
US20100281547 Selecting animals for desired genotypic or potential phenotypic properties Described are methods to select animals, such as mammals, particularly domestic animals, breeding animals or animals destined for slaughter, for having desired genotypic or potential phenotypic properties, in particular, related to muscle mass and/or fat deposition lean meat, lean back fat, sow prolificacy and/or sow longevity. Provided is a method for selecting an animal having desired genotypic or potential phenotypic properties comprising testing the animal, a parent of the animal or its progeny for the presence of a nucleic acid modification affecting the activity of an evolutionary conserved CpG island, located in intron 3 of an IGF2 gene and/or for the presence of a nucleic acid modification affecting binding of a nuclear factor to an IGF2 gene.
US20090263481 Levetiracetam formulations Pharmaceutical formulations comprising levetiracetam and having an inner solid phase and outer continuous phase, wherein one or both of the phases comprise at least one hydrophobic material, lipophilic material, or combination thereof.
EP1441667B1 Improved endoprosthetic device The invention relates to improved drug-delivery endoprosthetic device for insertion at a vascular site via catheter placement at the site, comprising: (a) a structural member into the upper and/or lower surface of which one or more micro-deepenings are engraved and/or on which a polymer member is carried, for co-expansion with the polymer member from a contracted state to an expanded state when the device is exposed to said stimulus, (b) optionally a polymer member capable of expanding from a contracted to a stable, expanded state when the polymer member is exposed to a selected stimulus, wherein the device can be delivered from a catheter, with the structural and the optional polymer members in their contracted states, and is adapted to be held in a vessel at the vascular target site by radial pressure against the wall of the vessel, with the structural and the optional polymer members in their expanded states; and wherein the micro-deepenings of said structural member and/or said polymer member comprise a pharmaceutical composition containing one or more active ingredients selected from the group consisting of agents to inhibit or at least reduce excessive proliferation of vessel wall cells, agents to enhance the downstream perfusion of tissue, agents to promote and/or to enhance the neo-formation of capillaries, agents designed to modulate the amount or activity of coagulation factors, agents to reduce the amount of Thrombin- and / or Fibrin-formation, embedded therein for release from the member, with such in its expanded state.
CA2245484C Novel urea derivatives Compounds of Formula I (see formula I) wherein R1 is hydrogen or lower alkyl, R2 is hydrogen or halogen and R3 is hydrogen or lower alkoxy, and their pharmacologically acceptable acid addition salts and pharmaceutical compositions containing these compounds and also processes for the preparation of these compounds.
WO2007005404A1 AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I. The present invention also provides methods for the use thereof to inhibit ß-secretase (BACE) and treat ß-amyloid deposits and neurofibrillary tangles
US20080207719 Treatment of Epilepsy The disclosure relates to a method for the inhibition of the development of epilepsy with an alpha2-adrenoceptor antagonist or a pharmaceutically acceptable salt or ester thereof.
US20130065834 Modulators of proteasome activity Methods of modulating proteasome activity, increasing life span and neurogenesis are provided herein.
WO2005005372A1 Compound having anti-hcv activity and process for producing the same A compound which has high HCV replication inhibitory activity and is hence useful in the prevention of and treatments for viral infectious diseases, especially liver diseases attributable to HCV infection; a process for producing the compound; an intermediate useful for the production; and a medicinal composition containing the compound. The compound is any of a compound represented by the formula (I): [wherein A represents -(CH2)n-, etc.; B represents -(C=O)-, etc.; D represents -(CH2)m-R', etc.; E represents hydrogen, etc.; G represents -(CH2)p-J, etc.; bond Q represents a single bond or double bond; and R1, R2, and R3 are the same or different and each represents hydrogen, etc.], a prodrug thereof, and a pharmaceutically acceptable salt of either.
CN1915223A Chewing tablet of compound aluminum magnesium hydroxide, preparation method and method for measuring quality A chewing tablet of compound aluminum magnesium hydroxide for treating gastric ulcer, duodenal ulcer, stomach-ache, gastritis, gastroxia, etc is prepared from 11 raw materials including hyoscine butylbromide, dioctyl hydrochloride, chlordiazepoxide, filler, disintegrant, etc. Its preparing process and its quality test method are also disclosed.
EP1955697B1 2-aminobenzamide derivatives as vanilloid receptor 1 (vr1) inhibitors useful for the treatment of pain or bladder function disorder Disclosed is a novel and excellent therapeutic or prophylactic agent for nociceptive pain, neuropathic pain, cancer pain, headache, bladder dysfunction or the like, which relies on a preventive activity on capsaicin receptor VR1 activation. It is found that a benzamide derivative having a benzene ring fused with a monocyclic ring on a nitrogen atom in the amide group and an amino group substituted by a lower alkylamino or cyclic group at a position adjacent to the amide group has a potent preventive activity on VR1 activation and an excellent pharmacological activity relying on the preventive activity, and therefore the derivative can be used as a good therapeutic or prophylactic agent for a VR1-related disease, such as nociceptive pain, neuropathic pain, cancer pain, headache and bladder dysfunction.
WO2006114371A1 Novel compounds for treating inflammatory diseases The invention relates to novel compounds of formula (1), heteroderivatives thereof, and pharmacologically compatible salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, that are suitable for treating respiratory or gastrointestinal complaints or illnesses, inflammatory diseases of the joints, skin or eyes, diseases relating to the peripheral or central nervous system, or cancerous diseases. The invention also relates to pharmaceutical compositions containing said compounds.
CN101700268A Liver protection soft capsules The invention relates to the field of health-care foods, in particular to liver protection soft capsules. The liver protection soft capsules are prepared from materials of kudzu root, vitamin E, salad oil and water. The liver protection soft capsules are prepared by the steps of mixing, stirring and filling to form capsule form. The liver protection soft capsules are characterized by comprising the following materials by weight percentage: 9-16 percent of kudzu root, 10-15 percent of vitamin E, 25-30 percent of salad oil and 45-50 percent of water. The liver protection soft capsules have low cost, simple and advanced production process and good effect, are easy to carry about, are suitable for different people, and have functions of neutralizing the effect of alcoholic drinks and protecting the liver.
EP2776031A1 N-methyl-2-[3-((e)-2-pyridin-2-yl-vinyl)-1h-indazol-6-ylsulfanyl]-benzamide for the treatment of chronic myelogenous leukemia The present invention relates to a method of treating chronic myelogenous leukemia in a subject comprising administering to the subject a compound, such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition comprising a compound such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]- benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.
US20080200559 Reducing fat; using ace inhibitor There is provided a method for altering the distribution of body mass by altering the distribution of body mass by decreasing overall percentage fat and/or increasing the proportion of lean mass to fat mass comprising administering to a subject one or more compounds having the ability to alter body mass composition and/or ACE inhibiting activity or a physiologically acceptable derivative or prodrug thereof.
US20120196874 Stilbene analogs and methods of treating cancer Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.
CN103479908A Ointment for treating burnt patients and preparation method thereof The invention discloses ointment for treating burnt patients. The ointment comprises the following active components by weight: 60-80g of red peony root, 40-60g of mint, 40-60g of puffball, 20-30g of buffalo horn, 40-60g of herba schizonepetae, 50-70g of purslane, 40-60g of dandelion, 50-70g of rhizoma phragmitis, 50-70g of dried cabbage leaf, 40-60g of bile arisaema, 10-20g of yellow lead, 40-60g of beewax, 40-60g of borneol, and 30-50g of saposhnicovia divaricata. The ointment can be used for solving the problems of local blood stasis and obstruction, meridian stagnation and toxic heat flourishing, and has good effects in activating blood circulation, removing stasis and dredging collaterals, clearing heat and toxicity and cooling blood, and treating burns; the effective rate is 93.6 percent, and the rate of favorable curative effect is 90.7 percent.
EP2782559A1 Pharmaceutical composition comprising myo-inositol and d-chiro-inositol This is a description of pharmaceutical compositions comprising inositol and D-chiro-inositol in specific ratios, useful in the treatment of PCOS and for improving oocyte quality in general.
WO2007129005A1 Aminoacid derivatives of thiazoles as inhibitors of pi3 kinase Compounds of formula (I) are inhibitors of PI3 kinase activity, and useful in treatment of, inter alia, autoimmune, inflammatory and proliferative diseases; wherein s is 0 or 1; U is hydrogen or halogen; X is -(C=O)-, or an optionally substituted divalent phenylene, pyridinylene, pyrimidinylene, or pyrazinylene radical, or a bond; P is optionally substituted C1-C6 alkyl and Z is -(CH2)Z-Y1-L1-R or Z is optionally substituted C1-C6 alkyl and P is -(CH2)Z-Y1-L1-R; and z, Y1, L1 and R are as defined in the claims.
EP1494665A1 Use of statins and other immunomodulatory agents in the treatment of autoimmune disease Methods are provided for the treatment of autoimmune diseases, by co-administering a statin and a second immunomodulaotry agent. The second immunomodulatory agent can be antigen-specific or non-antigen-specific.
US20110178108 Group of amino substituted benzoyl derivatives and their preparation and their use A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.
US7790773 a cyclopentene sugar amine derivative useful as beta -galactosidase stabilizing agent A carba-sugar amine derivative represented by the following formula (1) or (2) is used as the active ingredient of a β-galactosidase inhibitor or a glycolipid metabolic disorder treating agent. Wherein each of R1 and R2 independently represents H, an alkyl group, an acyl group, an aryl group or an aralkyl group, with the proviso that both are not H at the same time, and each of R3, R4, R5 and R6 independently represents a hydroxyl group or hydroxyl group having a substituent. Also, R7 represents an alkyl group, and each of R8, R9, R10 and R11 independently represents a hydroxyl group or a hydroxyl group having a substituent.
EP1927349A1 Composition for life extension and method of extending the life The present invention relates to a composition for life extension, comprising reduced coenzyme Q10 as an active ingredient, as well as relates to a method of extending a life span using the composition comprising reduced coenzyme Q10 as an active ingredient. In the present invention, it has been found that long-term ingestion of feed that contains reduced coenzyme Q10 enables the life span of senescence-accelerated model mice to be extended. No sign indicating toxicity is observed in the senescence-accelerated model mice that have been fed with reduced coenzyme Q10 over a long period. Based on these findings, it was found that the composition containing reduce coenzyme Q10 as an active ingredient has potential to be a composition for life extension with high safety, capable of being taken for a long period. The present invention provides a composition, which can extend the life span of humans or animals, enables them to spend active and healthy senectitudes and shows high safety during the ingestion over a long period.
EP2411529A2 N-linked glycan biosynthesis modulators Provided herein are N-linked glycan inhibitors, including modulators of N-linked glycan glycosylation, mannosidase, an N-linked glycan N-acetylglucosaminyl transferase, an N-linked glycan fucosyl transferase, an N-linked glycan galactosyl transferase, an N-linked glycan sialyl transferase, an N-linked glycan sulfotransferase, N-linked glycan glycophosphotransferase or a combination thereof
CN102225067B Pharmaceutical composition for treating stomach cancer The invention relates to a pharmaceutical composition for treating stomach cancer, which comprises tegafur, 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid or derivatives thereof. Studies of the invention show that in case of combination administration of 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid and derivatives thereof, tegafur and optional other medicines, the anticancer effect of tegafur is significantly enhanced. The pharmaceutical composition provided by the invention has a high inhibitory rate on stomach cancer in nude mice.
EP2762137A1 Use of myricetin or derivatives thereof as a cathepsin k inhibitor This invention is directed to a novel inhibitor on collagen degradation caused by the activity of a human cathepsin K rising. In particular, the inhibitor is myricetin or derivatives thereof. The invention also relates to use of the novel inhibitor to manufacture a medicament in a form of pharmaceuticals, foods, nutraceuticals or cosmetics for the prevention, amelioration and/or treatment of pathological symptoms or diseases associated with collagen degradation. Alternatively, the present invention is further directed to addition of the novel inhibitor to a medicament, food, nutraceutical or cosmetics used for the treatment, amelioration and/or prevention of the disease or pathological symptoms associated with collagen degradation by the increased human cathepsin K activety. The invention also provide the methods for treating, ameliorating and/or preventing the symptoms or diseases, comprising administering an effective amount of the medicament to a subject in need thereof.
WO2009153296A1 Pharmaceutical composition comprising a non-steroidal glucocorticoid receptor agonist in combination with a dual histamine antagonist An aqueous pharmaceutical composition which comprises a compound which is 1- {[3-(4-{[(2R)-4-[5-fluoro-2-(methyloxy)phenyl]-2-hydroxy-4-methyl-2- (trifluoromethyl)pentyl]amino}-6-methyl-1H-indazol-1-yl)phenyl]carbonyl}-D- prolinamide Formula (I) or a pharmaceutically acceptable salt thereof optionally in combination with a dual histamine antagonist or a pharmaceutically acceptable salt thereof, to processes for their preparation, and to their use in the treatment of various inflammatory and/or allergic conditions, such as allergic rhinitis.
US20080085878 Superoxide dismutase-2 expression and modulation for glaucoma diagnosis and therapy The present invention concerns a method for diagnosing or monitoring elevated intraocular pressure or glaucoma in a patient comprising providing a biological sample from the patient and measuring the expression level of a superoxide dismutase-2 (SOD-2) gene in the biological sample. The present invention also concerns methods for treating glaucoma or elevated intraocular pressure in a patient comprising administering to a patient an effective amount of an agent that modulates SOD-2 expression or SOD-2 activity.
CN101036639A Application of piperlonguminine and dihydropiperlonguminine in the preparation of the medicine for curing senile dementia An application of a piperlonguminine and a dihydropiperlonguminine for preparing a drug for treating senile dementia is disclosed in the invention, wherein, the piperlonguminine and the dihydropiperlonguminine having mass ratio of 1:1.08 are separated and extracted from pepper stem of FuJian. It is approved that the piperlonguminine and the dihydropiperlonguminine are active components for suppressing APP expression by the pepper stem via RT-PCR and Western Blot in the invention, with preferred drug concentration of 3.28 mu g/ml-6.56 mu g/ml. Accordingly, the piperlonguminine and the dihydropiperlonguminine has inviting developing prospect for preparing novel drug for treating the senile dementia.
EP2711017A1 Immunity inducing agent Provided is a novel immunity-inducing agent useful as a therapeutic and/or prophylactic agent for cancer. The immunity-inducing agent comprises as an effective ingredient(s) at least one polypeptide having immunity-inducing activity selected from the polypeptides (a), (b) and (c) below, and/or a recombinant vector(s) that comprise(s) a polynucleotide(s) encoding the at least one polypeptide, which recombinant vector(s) is/are capable of expressing the polypeptide(s) in vivo: (a) a polypeptide composed of not less than 7 consecutive amino acids in any one of the amino acid sequences of SEQ ID NOs:4, 2, 8, 10 and 12 in SEQUENCE LISTING; (b) a polypeptide having a sequence identity of not less than 85% to the polypeptide (a) and composed of not less than 7 amino acids; and (c) a polypeptide comprising the polypeptide (a) or (b) as a partial sequence thereof.
CN101317873B Hyperosteogeny ache-reliving plaster and preparation method thereof The present invention relates to a hyperosteogeny pain-relieving plaster which is made from the following raw material medicinesin weight proportions: 0.8 to 1.5 proportions of muskiness, 20 to 40 proportions of heracleum hemsleyanum michaux, 25 to 35 proportions of notopterygium root,30 to 50 proportions of mastic, 1.5 to 2.5 proportions of borneol, 15 to 30 proportions of myrrh, and 100 to 140 proportions of lard. The preparation method includes the steps that: impurities in the mastic and the myrrh are removed at first and the conglobation is smashed into particles, which are fried by mildfire till smoke goes out after being respectively put into a pan. When the surface assumes luster, the materials are taken out, cooled and ground into fine powder. The fine powder is screened by a screen with a filtering capacity of 120 meshes for standby; the muskiness and the borneol is ground into fine powder, which is then screened by a screen with a filtering capacity of 120 meshes for standby; the lard is roasted and the residue in the lard is filtered. Powder of the mastic, the myrrh, the notopterygium root and the heracleum hemsleyanum michaux is put into the cooled lard, which are mixed till the mixture becomes cream. Fine powder muskiness of the muskiness and the borneol is put into the cream and mixed, and then the obtained mixture is subpackaged. The hyperosteogeny pain-relieving plaster has remarkably curative effect in curing hyperosteogeny hernia of intervertebral disc, spondylitis ankylopoietica, heel bone spur and rheumatism and rheumatoid arthritis. The hyperosteogeny pain-relieving plaster is small in side effect with a curative ratio reaching 90 percent and 98.33% an effectiveness ratio.
WO2010088225A2 Regulation of mammalian keratinous tissue using skin and/or hair care actives Personal care compositions containing an active selected from the group consisting of phlorogine, phlorgine BG, deoxyArbutin, sucrose dilaurate, bakuchiol, pyrenoine, millet, arlatone dioic acid, cinnamic acid, ferulic acid, achromaxyl, methyl nicotinamide, oil soluble licorice extract, folic acid, undecylenic acid, zinc undecylenate, L-tryptophan, thiamine HCl, hexylresorcinol, lipidami red vine, dragosine, methyl gentisate, inositol, symdiol 68, laminaine, their salts, their derivatives, their precursors, and/or combinations thereof. Methods for regulating the condition of mammalian keratinous tissue by topically applying the personal care compositions are also provided.
CN103086921A 2-(4-aryloxyphenoxy)alkylamide and application thereof The invention relates to 2-[4-(benzoxazol-2-yloxy)phenoxy]alkylamide represented by a chemical structural formula I or an optical isomer thereof, wherein R1 is selected from H, C1-C1 alkyl, and C3-C4 straight-chain or branched-chain alkyl; R2 is selected from allyl, propargyl, halogenated allyl, and halogenated propargyl; X1-X6 are selected from hydrogen, C1-C2 alkyl, trifluoromethyl, fluoro, chloro, bromo, nitro, or trifluoromethoxy. The invention also relates to the application of the 2-[4-(benzoxazol-2-yloxy)phenoxy]alkylamide or the optical isomer thereof in preparing anti-lung-adenocarcinoma medicines.
CN102805725A Azlocillin sodium medicinal composition for injection and preparation method for azlocillin sodium medicinal composition for injection The invention discloses an azlocillin sodium medicinal composition, namely azlocillin sodium nanoparticle injection. The azlocillin sodium nanoparticle injection consists of azlocillin sodium, a carrier material, stabilizer and excipient, and the effective average particle size of nanoparticles is 10 to 200nm. The invention discloses a preparation method for the injection; and the method comprises the following steps of: mixing the azlocillin sodium and the stabilizer in water for injection, adjusting pH value, and adding the carrier material and the excipient to obtain the azlocillin sodium nanoparticle injection. The injection has the advantages of high redissolution performance, excellent stability, high medicine loading capacity and the like, and the process is suitable for industrial large-scale production.
EP0842923B1 Pyrrole derivatives and medicinal composition A medicinal composition which comprises as the active ingredient a pyrrole derivative represented by general formula (1), a pharmaceutically acceptable salt thereof, or a solvate of either of the same, wherein R1 represents hydrogen or alkoxycarbonylamino; R2 represents alkyl, optionally substituted aryl, an optionally substituted aromatic heterocycle, unsubstituted amino, monoalkyl-substituted amino, dialkyl-substituted amino or optionally substituted cyclic amino; R3 represents cyano or carbamoyl; R4 represents hydrogen or alkyl; E represents alkylene; q is 0 or 1; and A represents methyl, optionally substituted aryl or an optionally substituted aromatic heterocycle. The medicinal composition is efficacious in treating frequent urination or urinary incontinence.
CN102757299A Protein tyrosine phosphatase inhibitor The invention relates to a compound which plays a role in inhibiting protein tyrosine phosphatase, and the inhibiting effect of a composition containing the compound on protein tyrosine phosphatase. The compound can be applied to preparation of a medicament for treating diabetes mellitus II or obesity caused by high expression of in-vivo protein tyrosine phosphatase.
WO2010115932A1 Combination for the treatment of bone loss The invention provides a novel treatment regime for bone loss, such as that which occurs in osteoporosis patients. In said regime the patients arc provided with a single high dose of a bone anabolic agent and a single high dose of a bone resorption inhibitor.
US7776902 N-[4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenylsulfonyl]-4-nitrooxybutanamide, used for the treatment of inflammatory, cardiovascular, gastrointestinal, respiratory and nervous system disorders, as analgesics, antipyretics and antocoagulants or for organ and tissue preservation New compounds able to release COX-2 inhibitors and NO having formula (I): M-T-YA—NO2 (I) for the treatment and/or prophylaxis of inflammatory processes.
US20050063909 Drug and adverse-effect agent coated with inner acid-soluble layer and outer base-soluble layer; sustained release; multilayer tablets; for treatment of pain with opiod analgesics The present invention provides an oral dosage form comprising a first composition and a second composition. The first composition comprises an effective amount of a therapeutic agent and the second composition comprises an effective amount of an adverse-effect agent. The adverse-effect agent is covered with a coating that is substantially insoluble in the gastrointestinal tract. In one embodiment, the adverse-effect agent is coated with an outer base-soluble layer and an inner acid-soluble layer. The therapeutic agent can be uncoated or can be coated with a coating having an outer acid-soluble layer and an inner base-soluble layer. The dosage form discourages administration of the therapeutic agent by other than oral administration.
WO2011107617A1 Liquid ibuprofen/codeine pharmaceutical composition for oral administration, the method for preparation thereof and use thereof The present invention relates to a novel liquid pharmaceutical composition that contains ibuprofen in the form of a salt formed with a basic amino acid and codeine or a pharmaceutically acceptable codeine salt, for oral administration, and in particular the composition contains an ibuprofen salt or a basic amino acid such as arginine, lysine or mixtures thereof. Furthermore, the invention relates to a method for preparing said pharmaceutical composition and also the use thereof, preferably in paediatrics, for the manufacture of a drug that can be used to treat moderate-to-severe pain, inflammation, fever and/or other illnesses in which ibuprofen and/or codeine are traditionally used principally as analgesic. The composition of the invention exhibits good stability after three years under different temperature and relative humidity conditions.
CA2409069C Hydrogel composition for transdermal drug delivery The present invention relates to a hydrogel composition for transdermal drug delivery, more specifically to a hydrogel composition for transdermal drug delivery containing acrylate polymers like acrylic acid polymer, methacrylic acid polymer, alkyl acrylate polymer, alkyl methacrylate polymer or copolymers thereof as compatibilizers which enable both hydrophilic and lipophilic permeation enhancers to be applicable in the hydrogel composition in order to effectively control skin penetration of drugs.
US8138200 Compositions and methods for double-targeting virus infections and targeting cancer cells The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
CN101264068A Ciclesonide dry powder inhalant and preparation thereof The invention relates to a ciclesonide dry powder inhaler as well as a preparation method, which takes the ciclesonide as the medicinal active component and forms a medicinal composition with acceptable accessories in pharmacy. The formulations supplying through mouth, such as dry powder inhaler and aerosol prepared according to the technical means of the invention, have the advantages of rapid effect, quick action and convenient use. The ciclesonide dry powder inhaler can be used for curing different classes of asthma.
EP1634595A1 N-Phenylbenzamide derivatives as drugs for the treatment of Chronic Obstructive Pulmonary Disease (COPD) The invention relates to the use of a pharmaceutically active derivative of N-phenylbenzamide of Formula (I) or of a pharmaceutically acceptable salt thereof, for preparing a medicament for the therapeutic treatment of Chronic Obstructive Pulmonary Disease (COPD). Compounds of Formula (I): wherein R1 is cyano, nitro, halogen, hydroxy, C1-C4 alkyl, methoxy or tetrazol-5-yl group, R2 is hydrogen, hydroxy or methoxy, R3 is a tetrazol-5-yl group or hydrogen, R4 and R5 are hydrogen if R3 is tetrazol-5-yl group, or R4 and R5 are independently selected from the group consisting of carboxy, methoxycarbonyl, ethoxycarbonyl and carbamoyl if R3 is hydrogen, and R6 is hydrogen or methyl.
CN103183655A Nor-sesquiterpenoid compound as well as preparation method and application thereof The invention discloses a nor-sesquiterpenoid compound as well as a preparation method and application thereof. The compound provided by the invention is extracted from the rice fermented product of edible mushroom flammulina velutipes, and has a structural formula as shown in formula I: FORMULA, wherein both R1 and R5 are selected from double-bond oxygen, hydroxyl group or hydrogen; C1 and C2 or C2 and C7 form a carbon-carbon single bond or carbon-carbon double bonds and are not carbon-carbon double bonds simultaneously; when C1 and C2 or C2 and C7 form a carbon-carbon single bond, R2 is hydrogen or hydroxyl group; when C1 and C2 or C2 and C7 form carbon-carbon double bonds, R2 is inexistent; when C1 and C2 form a carbon-carbon single bond, R3 is double-bond oxygen, hydroxyl group or hydrogen; when C1 and C2 form carbon-carbon double bonds, R3 is hydroxyl group or hydrogen; C5 and C6 form a carbon-carbon single bond or carbon-carbon double bonds; when C5 and C6 form a carbon-carbon single bond, R4 is hydrogen or hydroxyl group; and when C5 and C6 form carbon-carbon double bonds, R4 is inexistent. Experiments prove that the compound can be used as a cell proliferation inhibitor or an anti-tumour agent. (FORMULA I).
US20100160454 Use of 1,2-cyclohexanedimethanol, 1,4-cyclohexanedimethanol, or 2,2,4,4-tetramethyl-1,3-cyclobutanediol as microbiocides or to prevent biofilms in water, for example use in personal care applications, in fuels, or on moldings or composites Antimicrobial agents, products and compositions incorporating the agents, and methods of using the compositions and products are provided. The antimicrobial agents comprise 1,2-cyclohexanedimethanol, 1,4-cyclohexanedimethanol, 2,2,4,4-tetramethyl-1,3-cyclobutanediol, or mixtures thereof. These agents have surprisingly been found to inhibit microbial growth at a much lower concentration than other glycols with known antimicrobial activity.
US20100184849 Urea oligomers, their preparation process and pharmaceutical compositions containing them A method for treating a cytotoxic disease by administrating compounds having a general formula X-(A)n-Y, wherein: n varies between 6 and 20; X denotes a hydrogen atom, an RaCO, RaOCO, RaNHCO or RaSO2 group, Ra being an alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl group, the groups being substituted or not, on condition that X is different from H when n is equal to 6; A denotes either a group having formula (I) or (II), wherein Ri is a hydrogen atom, an amino acid side chain, an alkyl, alkenyl, alkynyl, aryl, aralkyl or heteroaryl group, said groups being substituted or not, i being an integer of between 1 and n; Y is an NRbRc, Rb and Rc group having the same meaning as given earlier for Ra.
EP1212296B9 Phosphate mimics and methods of treatment using phosphatase inhibitors The invention relates to trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and the physiologically acceptable salts and the prodrugs thereof. These compounds are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer, diabetes, immuno-modulation, neurologic degenerative diseases, osteoporosis and infectious diseases. The invention also relates to the use of compounds containing fluoromethyl sulfonyl groups as phosphate mimics. These mimics may be used to inhibit, regulate or modulate the activity of a phosphate binding protein in a cell.
US20110144102 Calcimimetic compound for use in the treatment of epithelial injury This invention relates generally to the field of medicine and, more specifically, to methods for treating epithelial injury, in particular, due to ischemia, hypoxia, trauma, chemolytics or radiation exposure.
CN101354397A Strategy for retroviral immunotherapy The invention points out generating at least two immune cell colonies at responding to retrovirus infecting mammals. In particular, the immune system of the mammals infected by the retrovirus can enhance the immune response of the retrovirus through a group of cells generally named as effector cells, however, the second immune cell colony is generated synchronously to regulate the effector cells generally named as regulation cells (or suppressor cell), so as to restrict the capability of the mammals for effectively controlling or eliminating the retrovirus infection. Therefore, the invention uses these observation results to provide a method for treating the mammals infected by the retrovirus. Moreover, the invention has found that an acute inflammatory index can be used for detecting and monitoring the response of the effector cells to the retrovirus antigen.
US20070275994 Novel Antinfective Compounds The present invention describes novel antiinfective compounds of formula (I), process for their preparation and pharmaceutical compositions containing them.
EP2651939A1 SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-a]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.
WO2006138230A3 The preparation and use of protease inhibitors Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein, X is -C(R3 R4)-; Y is -N(R5)-; Z is -C(=N-R5’)-; and R1, R2, R3, and R4 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.
EP2145883A1 Dibenzyl lipoic acid derivatives and their use in treatment of disease The invention provides a method of inhibiting proliferation of diseased cells by contacting the diseased cells with an effective amount of a reagent that inhibits PDC specifically in said diseased cells.
WO2012173383A3 Skin composition for external use containing cryptotanshinone as active ingredient The present invention provides a skin composition for external use containing cryptotanshinone, an isomer thereof, a precursor thereof, a salt thereof, a hydrate thereof, or a solvate thereof as an active ingredient. The composition according to the present invention has the effects of suppressing skin aging, smoothing skin wrinkles, skin whitening, skin moisturizing, improving atopic dermatitis, and improving skin tone and skin transparency.
US20090149418 Antimicrobial preparations using polysaccharide gel from durian fruit-rind A water-soluble polysaccharide gel having good gelling property and good antimicrobial activity was extracted from fruit-rind of durian (Durio zibethinus Murr.) comprises steps of boiling dried fruit rind with 25-30 volumes by weight of water, filtering, repeating boiling residue 1-2 times with 15 volume by weight of water. Filtrates were pooled and concentrated by rotary evaporating at 70° C. under reduced pressure and precipitating using acidified aqueous ethanol, collecting precipitate, spray-drying or drying and pulverizing. Pharmaceutical preparations were prepared using the polysaccharide gel such as anti-acne preparations, alcohol-free hand sanitizer preparation and wound antibacterial gel preparation.
EP0954278B1 Pharmaceutical compositions containing kukui nut oil The present invention provides pharmaceutical compositions comprising an effective amount of dermopharmaceutical active agent, kukui nut oil and a pharmaceutically acceptable base which comprises ingredients selected from the group consisting of propylene glycol, glycerin, xanthin gum, methyl paraben, propyl paraben, stearic acid, menthyl lactate, cetearyl alcohol (and) ceteareth 20, polyoxyl 40 stearate, glyceryl stearate (and) PEG-100 stearate, isopropyl myristate, isopropyl alcohol, oleyl alcohol, oleic acid, dimethicone, or C12-C15 alcohols benzoate and purified water. The inclusion of kukui nut oil acts in synergy as an adjunct to the therapeutic agent to promote the alleviation of the medical condition being treated.
US20120251522 Targeted delivery of therapeutic agents with lyophilized matrices Embodiments of surgical grafts, and methods, for the delivery of therapeutic agents to a target tissue via acellular matrices, are described. In some embodiments, nonviable matrices are successful in preventing or lessening adhesion formation by guiding tissue repair and remodeling, while also providing the target tissue with therapeutic agents that can act as repair and remodeling factors. An exemplary method to modulate flexor tendon healing and provide elimination or reduction of fibrotic adhesions involves loading a freeze-dried flexor digitorum longus allograft with recombinant adeno-associated viral (rAAV) vectors for the targeted and transient expression of growth/differentiation factor 5 (GDF5).
US20110269820 Spinal muscular atrophy treatment via targeting smn2 catalytic core The present invention is directed to methods and compositions for blocking the effect of the intronic inhibitory splicing region of intron 7 of the SMN2 gene. The compositions and methods of the instant invention include short oligonucleotide reagents (e.g., oligoribonucleotides) that effectively target sites in the SMN2 pre-mRNA, thereby modulating the splicing of SMN2 pre-mRNA to include exon 7 in the processed transcript. The short target regions are 8-mers and 5-mers and also include the identification of a single nucleotide base that is essential for initiating a long distance stearic inhibitory interactions as well as novel targets distant from intron 7 which block the intronic inhibitory splicing of the same. These short target regions and concomitant inhibitory blocking oligonucleotides are less expensive and easier to manufacture and are small enough to cross the blood brain barrier.
CN1861084A Compound fluorophenylnico injection, prepn. method and use thereof A compound florfenicol injection for treating the pneumonia and bacterial lung infection of pig is prepared from florfenicol, doxycycline, dimethyl formamide, magnesium dichloride, polyvinyl pyrrolidone, trimethoprim and propanediol. Its preparing process is also disclosed.
US20080262014 Use of Camptothecin Derivatives for the Treatment of Proliferative Diseases in a Fixed Dosing Regimen Topoisomerase I inhibitors are administered for the treatment of proliferative diseases according to a once every three day fixed dosing regimens. Furthermore, the invention provides the use of topoisomerase inhibitors to manufacture a medicament which can be used in a fixed dose treatment regimen.
US20110021577 Aryloxy amine compounds and their use as sodium channel modulators The present invention relates generally to the field of therapeutic treatment and compounds having utility therefor, in particular the therapy or management of conditions associated with excessive, unwanted or undesirable sodium ion passage through cellular membranes via voltage-gated sodium channels. In one embodiment the invention is concerned with the treatment of neuropathic pain. The invention contemplates to aryloxy-substituted amines, as sodium channel blockers or modulators. In further embodiments, the invention also relates to compounds which may advantageously have dual sodium channel blocker/modulating and antioxidative (free-radical scavenging) effects. Methods for their manufacture and compositions containing the compounds are also contemplated.
WO2008059214A1 Bisamlde derivatives and use thereof as fatty acid synthase inhibitors A compound of formula I, or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.
CN102670584A Application of gallocatechin gallate in preparation of benign prostatic hyperplasia resistant medicament The invention discloses application of gallocatechin gallate in preparation of a benign prostatic hyperplasia resistant medicament. Influence on prostate weight and prostate indexes of a rat and pathological change of prostate tissues are observed through a testosterone propionate induced castrated rat prostatic hyperplasia model by using the gallocatechin gallate as a treatment medicament. Research results show that the gallocatechin gallate can remarkably reduce the prostate weight and the prostate index of a model animal and improve the pathological symptoms of the prostate tissues.
WO2008101943A1 Pharmaceutical metformin hydrochloride formulation and tablet comprising said formulation A formulation is described comprising micronized metformin HCI useful for the preparation of pharmaceutical tablets by simple compression.
CN1830453A Preparation method of vitamin medicinal composition A freeze-dried powder injection of composite vitamins containing 12 components for treating the diseases caused by biochemical reactions in human body is prepared from said composite vitamins through depositing in water, cold storage, ultrafiltration, further preparing in dark condition and N2 atmosphere, pouring in containers, freeze drying and sealing.
US20110218221 Novel histone deacetylase inhibitors, process for preparation and uses thereof The present invention relates to compounds represented by formula (I) or composition comprising at least one of such compounds, which are inhibitors of histone deacetylase. The detailed description of these compounds is disclosed in the Description. These compounds and the composition comprising the same may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities.
WO2009061595A1 Compounds for inhibiting ksp kinesin activity The present invention relates to compounds of Formula (I), below, (wherein R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
CN102813626A Amorphous form cefmenoxime hydrochloride compound combination for injection The invention discloses an amorphous form cefmenoxime hydrochloride compound combination for injection. The amorphous form cefmenoxime hydrochloride compound combination is composed of raw material cefmenoxime hydrochloride and auxiliary material L-arginine and is characterized in that the raw material cefmenoxime hydrochloride is an amorphous form compound, and every 1000 cefmenoxime hydrochloride combination includes: 500-2000g of cefmenoxime hydrochloride calculating by cefmenoxime and 300-1200g of L-arginine. A preparation method of the amorphous form cefmenoxime hydrochloride compound combination for injection includes: weighing amorphous form cefmenoxime hydrochloride and L-arginine in a 100-level clean area, mixing the amorphous form cefmenoxime hydrochloride and the L-arginine according to proportion in a prescription, split charging the mixture in tubular bottles after the content of the mixture is measured to be qualified, pressing, rolling, performing lamp detection, and labeling and packaging after the detection is qualified to obtain the amorphous form cefmenoxime hydrochloride compound combination for injection.
US20070276141 Preparation of Pharmaceutical Salts of [1,4] - Bipiperidine The invention provides anhydrous and hydrated forms of sodium salt of N-[[4-(3,4-dichlorophenoxy)[1,4′-bipiperidin]-1′-yl]carbonyl]-4-methyl-benzenesulfonamide and crystalline forms of N-[[4-(3,4-dichlorophenoxy)[1,4′-bipiperidin]-1′-yl]carbonyl]-4-methyl-benzenesulfonamide; and such compounds are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis.
US20070254023 Perorally Administrable Antimicrobial Composition The invention relates to medicine and the chemical and pharmaceutical industry, in particular to antibiotic preparative forms. The inventive antimicrobial composition contains antibiotic selected from a group of lincosamides, broad-spectrum penicillins, cephalosporins, macrolides, tetracyclines, and lactulose at the active component ratio of 1:1-1:100. The mean particle size of lactulose ranges from 100 nm to 200 μm. Said composition is embeddable in a solid state and in the form of a syrup or a suspension. When applicable, pharmaceutically acceptable excipients are added into the composition in such a way that it takes a form acceptable for peroral administration.
CN101781227A 2-N-[(1R, 2R)-1, 3-dihydroxy-1-phenylpropyl]-fatty amide compound, preparation and application thereof The invention discloses a 2-N-[(1R, 2R)-1, 3-dihydroxy-1-phenylpropyl]-fatty amide compound, preparation and application thereof. The compound is a small molecule nerve growth factor ceramide analogue which is prepared by reforming the structure of (1R, 2R)-2-amido-1, 3-benzene propylene glycol used as a raw material. The structural formula is shown in the specification of the invention, wherein R=amyl, heptyl, nonyl, undecyl, tridecyl, pentadecyl or heptadecyl. The preparation method comprises the steps of: adding quantitative different p-nitrophenyl fatty acid ester to an anhydrous THF solution of the (1R, 2R)-2-amido-1, 3-benzene propylene glycol; stirring at room temperature; reacting for 48 hours; finishing a TLC track detection reaction; evaporating reaction mixtures under a decompression condition; and taking solution of chloroform and acetone which are mixed in the proportion of 85: 15 to 80: 20 to separate and purify residues by silica gel chromatographic columns to obtain the 2-N-[(1R, 2R)-1, 3-dihydroxy-1-phenylpropyl]-fatty amide compound. The compound can be used as a nerve growth factor and a regulating agent in immune reactions.
US20100240714 Oral composition for dental purposes A dental composition for oral use, containing a phosphorylated saccharide (a), a cationic bactericidal agent (b) and a solvent (c). By using the dental composition for oral use of the present invention, the adhesion of the bacteria in the oral cavity to the surfaces of the teeth can be suppressed for a long period of time; therefore, the dental composition for oral use can be suitably used for, for example, a mouse-wash agent, a dentifrice agent, a gargling agent, a mouse spray, a coating agent or a bonding agent to tooth surface or a dental prosthetic, a hypersensitive inhibitor, a therapeutic agent for periodontal diseases, that is applied to a periodontal pocket, or the like.
US20110201596 Methods for Providing Oxidatively Stable Ophthalmic Compositions This invention relates to a process for improving the stability of an ophthalmically compatible solution comprising at least one oxidatively unstable ophthalmic compound.
EP1233964B1 New use and novel n-azabicyclo-amide derivatives This invention relates to new use of a compound of general formula (I) wherein: A represents (II), (III), (IV), (V), (VI); D represents oxygen, or sulfur; R1 represents hydrogen or methyl; R2 represents hydrogen, or C¿1?-C4 alkyl; and R?3¿ represents (A), (B), (C), or an enantiomer thereof, and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment of prophylaxis of psychotic disorders and intellectual impairment disorders.
WO2011040600A1 NOVEL ANTIBACTERIAL AGENT TARGETING RESPONSE REGULATOR WaIR(YycF) Disclosed are a compound or a pharmaceutically acceptable salt, solvate or N-oxide thereof, and an antibacterial agent which uses the above and which is effective against gram-positive bacteria. The compound is represented by formula (I) [wherein R1 represents a 6-10 membered-ring aryl substituted by a C1-6 haloalkyl, and R2 and R3 each independently represent hydrogen, a C1-6 alkyl, a C3-6 cycloalkyl, or a C1-6 alkyl substituted by a 6-10 membered-ring aryl, and X represents oxygen or sulphur].
EP1337521B1 Salts of an isothiazole-4-carboxamide and their use as anti-hyperproliferation agents The invention relates to hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salt forms of 3-(4-bromo-2.6-difluoro-benzyloxy)-5-[3-(4-pyrrolidin-1-yl-butyl)-ureido]-isothiazole-4-carboxylic acid amide having the following formula: formula 1. The invention also relates to pharmaceutical compositions containing the hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salts of formula 1. The invention further relates to methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above salts and to methods of preparing the crystal forms of the above slats.
CN101269025A Famciclovir sustained-release dropping pill and preparation method thereof The invention discloses an antivirus drug compound and particularly relates to an oral pharmaceutical preparation adopting famciclovir as the ingredient and being prepared jointly with the medicinal carrier used as the stroma. The antivirus drug compound aims to supplement the deficiency of the prior antivirus oral pharmaceutical preparation and provide a sustained-release famciclovir dropping pill which has high bioavailability, fast effect, high drug content, low frequency of drug taking, full release, convenient drug taking, low cost and absence of contamination during the production. The sustained-release famciclovir dropping pill adopts famciclovir as the ingredient and is prepared jointly with the medicinal carriers of mixing hydrophilic frame ingredients and hydrophobic frame ingredients as the stroma.
WO2012149602A1 Multiple myeloma treatment A method of treating a subject presenting with multiple myeloma at a stage characterized by an increase in the prevalence of MM cells that (1) are IL-6 non-responsive and/or (2) have a CD45- phenotype, comprising administering to the subject an amount of a compound of formula Ib.
US20090074883 Multivitamin and Mineral Compositions for Individuals Having Renal Disease The present invention relates to oral compositions which are useful for nutrient supplementation. The dietary supplements and pharmaceutical products and methods of the present invention are particularly useful in the treatment of patients in various stages of chronic kidney disease and supplementing levels of physiological anti-oxidants, vitamins, and minerals in subjects requiring dialysis therapy.
US20060204471 Compositions and regime/regimen for treating the adverse signs of cutaneous skin aging Cosmetic/dermatological compositions suited for combating the adverse signs of cutaneous skin aging, notably for maintaining and/or enhancing the thickness of the skin, particularly the thickness of the epidermis, comprise a thus-effective amount of at least one substance/species which is active with respect to the trophicity of the cutaneous nerves and/or at least one neurostimulant and/or at least one neuroactivator and/or at least one neuromediator, formulated into a cosmetically/dermatologically acceptable vehicle, diluent or carrier therefor.
US8371292 Use of ciclesonide for the treatment of respiratory diseases The invention relates to new method of treatment of respiratory diseases, in particular the treatment of asthmatic children.
WO2014138712A1 Co-administration of steroids and zoledronic acid to prevent and treat osteoarthritis A combination therapy for treating osteoarthritis is disclosed. The combination therapy includes the co-administration of a steroid and Zoledronic Acid. The coadministration of a steroid decreases the production of cytokines, and, therefore, decreases the pro-inflammatory effects of Zoledronic Acid. The co-administration of Zoledronic Acid with steroids treats osteoarthritis, and helps to prevent the onset of osteoarthritis in patients at risk for osteoarthritis.
WO2007057873A3 Novel compositions to improve gut health and animal performance and methods of making the same The present invention relates to compositions comprising at least about 8% β-glucans and /or at least about 8% α -fucans which has a prebiotic effect and act as a replacement for in- feed antibiotics. The present invention also relates to extraction methods to obtain such extracts and various uses for the compositions comprising β-glucans and /or α -fucans.
CN103006542A Platycodin D sperm-killing contraceptive suppository for external use and placing device thereof The invention discloses a platycodin D sperm-killing contraceptive suppository for external use. The contraceptive suppository is characterized in that the active ingredient of the suppository is platycodin D diluent; the platycodin D diluent is different concentrations of physiological saline solution of platycodin D extracts; and the suppository is solid at normal temperature. When the contraceptive suppository is used, the contraceptive suppository is quickly dissolved in vaginas at body temperature, is in a semi-liquid state and can quickly kill sperms after being in contact with the sperms and deactivate the sperms, thus playing a role in contraception. The invention also discloses a matched placing device of the contraceptive suppository. The contraceptive suppository has a good contraceptive effect and can avoid unplanned pregnancy.
CN1634129A Sustained release high calcium formulation and preparation process thereof Disclosed is a sustained release high calcium formulation and preparation process, wherein the formulation comprises calcium as active component, slow release material coated outside the active component and adjuvant by the weight ratio of 90-110 : 5-20 : 131-165, the slow release material includes any one to four from acrylic resin, methyl hydroxypropylcellulose, ethyl cellulose, cellulose acetate-phthalate, and polyvinylpyrrolidone.
WO2008044632A1 1-naphthyl alkylpiperidine derivative Disclosed is a pharmaceutical composition comprising a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient, which has an antagonistic activity on a melanin-concentrating hormone receptor. The pharmaceutical composition is useful, due to its antagonistic activity on a MCH receptor, for the prevention or treatment of a disease such as depression, anxiety disorder (e.g., generalized anxiety disorder, post traumatic stress disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder), attention deficit disorder, mania, manic-depressive disorder, schizophrenia, mood disorder, stress, sleep disorder, attack, memory dysfunction, cognitive impairment, dementia, amnesia, delirium, mental deterioration, obesity, eating disorder, appetite disorder, hyperphagia, bulimia, cibophobia, diabetes, a cardiovascular disease, hypertension, dyslipidemia, cardiac infarction, movement disorder (e.g., Parkinson's disease, epilepsy, convulsion, tremor), drug abuse disorder and drug addiction.
US20050281794 comprising a catechin (epigallocatechin gallate), an anti-oxidant (ascorbic acid), proline and lysine; cancer The present invention relates to a composition comprising a catechin compound, ascorbic acid, proline and lysine. The present invention also relates to a method for treating neoplastic disease using a composition comprising a catechin compound, ascorbic acid, proline and lysine.
CN102670634A C-glycosylflavones composition, preparation method and application thereof The invention discloses a C-glycosylflavones composition. The composition is extracted from plants of genus Trollius, and mainly contains orientin, vitexin, or vitexin esters and orientin esters. The invention also discloses a preparation method of the C-glycosylflavones composition. The preparation method is characterized by comprising extracting Trollius Chinensis Bge., performing macroporous resin column chromatography, and performing selective gradient elution with ethanol-water mixed solvent. The macroporous resin is preferably weak polarity macroporous resin. The C-glycosylflavones composition has pharmacological effects in resisting oxidation and inflammation, and inhibiting bacterial infection; and can be applied as ingredient of drugs and functional foods.
CN102309714A Capsule for invigorating stomach and smooth intestine The invention provides an enteric capsule for treating acute and chronic enteritis, ulcerative enteritis, erosive enteritis and deficiency cold of spleen and stomach. The capsule has effects of reinforcing the vital energy and consolidating the constitution, tonifying middle-jiao and qi, inducing diuresis with bland drug, removing necrosis and promoting granulation, and can reach focus of a disease directly, remove damp and hot in gastrointestinal tract in a shortest time, rapid alleviate symptoms of loose stools, frothy stools, puriform stools, jelly stools, and tenesmus and restore ulcer and erosive surfaces, so as to promote rapid renewal of normal mucous membrane of the gastrointestinal tract.
CN103156917A Preparation method of Sanhua bone setting powder The invention provides a preparation method of Sanhua bone setting powder, which particularly relates to the preparation of nux vomica so as to reduce the toxicity of the nux vomica in the Sanhua bone setting powder. According to the preparation method, the nux vomica is processed by microwave irradiation, so that brucine and vauqueline in the nux vomica are converted into respective derivatives. The preferable method is as follows: the nux vomica is oxidized by using peroxide solution. The preparation method is simple, and the stability of the quality of the Sanhua bone setting powder can be kept.
CN101590045A Medicine combination containing amlodipine besy and naftopidil and application thereof The invention discloses an application of a medicine combination, namely the application of the combination containing amlodipine besy and naftopidil of officinal dosage and a carrier acceptable in terms of pharmacy for preparing medicine for treating high blood pressure or/and diseases related to prostatic hyperplasia. The invention also relates to the application of the medicine combination in preparing medicine for preventing, curing and delaying high blood pressure and/or diseases related to benign prostatic hyperplasia. With the implementation of the invention, the medicine combination with special usage not only has precise curative effect but also improves the compliance of the patients, brings convenience to medicine taking, reduces medical expenses and enjoys good market prospect.
EP2699218A1 Use of a combination of carotenoid, phytoestrogen and vitamin c for the prevention and/or treatment of pigmentation disorders The present invention relates to the use, for preventing and/or treating pigmentation disorders, for the preparation of a cosmetic composition suitable for orally administering a dailydose of from 1 to 25 mg of a carotenoid, from 10 to 300 mg of a phytooestrogen and from 10 to 1000 mg of vitamin C.
CA2501610C Epothilone derivatives for the treatment of multiple myeloma The present invention relates to a method of treating a warm-blooded animal, especially a human, having myeloma, especially myeloma which is resistant to conventional cytotoxic chemotherapy, comprising administering to said animal a therapeutically effective amount of an epothilone, especially an epothilone of formula (I), to a combination comprising an epothilone, for simultaneous, separate or sequential use; and to a pharmaceutical composition and a commercial package comprising said combination.
US20050075271 Crystalline beta2 adrenergic receptor agonist The invention provides a crystalline salt form of a novel β2 adrenergic receptor agonist. The invention also provides pharmaceutical compositions comprising the crystalline form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt form to treat diseases associated with β2 adrenergic receptor activity, and processes useful for preparing such a crystalline compound.
US20080214673 e.g. Furan-3-carboxylic acid [(1R,3R)-3-(3-chloro-phenylethynyl)-3-hydroxy-cyclohexyl]-amide; metabotropic glutamate receptors modulator/antagonist;anxiolytic agent, antidepressant; amidation of amine-compounds The invention provides compounds of formula (I) wherein R1 represents hydrogen or alkyl; R2 represents an unsubstituted or substituted heterocycle or R2 represents an unsubstituted or substituted aryl; R3 represents alkyl or halogen; X represents a single bond or an alkandiyl-group, optionally interrupted by one or more oxygen atoms or carbonyl groups or carbonyloxy groups in free base or acid addition salt form, processes for their preparation and their use as pharmaceuticals.
WO2006117977A1 Process for production of carbostyril compound Disclosed is an improved process which can produce a carbostyril compound of the formula (1) or a salt thereof, which is useful as a pharmaceutical agent, more safely with higher efficiency. An improved process for producing a carbostyril compound comprising the steps of adding a high boiling solvent to a compound of the formula (4) and refluxing the resulting mixture under heating in hydrochloric acid to produce a compound of the formula (5) safely and acylating the compound of the formula (5) to produce a carbostyril compound of the formula (1).
CN101152206A Mixed liquor having beauty treatment function and method for producing the same The invention provides imitation liquor with the function of cosmetology and the preparation method. The invention is characterized in that the liquor with a concentration with 10 to 45 degrees contains hyaluronic acid and one liter of the liquor contains 90 to 270 mg of hyaluronic acid component. And the imitation liquor containing 10 to 45 degrees hyaluronic acid also contains: procyanidine, and one liter of the imitation liquor contains 285 to 665mg of procyanidine component; and/or contains safflower extract and the content of the safflower extract active function component in one liter of the imitation liquor contains equals 3.0 to 6.0g active function component contained in dry basis safflower; and/or soybean isoflavone and one liter of the imitation liquor contains 72 to 135mg of soybean isoflavone effective component. The imitation liquor of the invention enables the function components exist stably and is capable of improving the absorption of function components by human body, thereby having the functions of moistening, moisture retention and cosmetology and is especially suitable for ladies.
CN102115470A Pyrimidine small-molecular compounds, and preparation method and application thereof The invention discloses novel pyrimidine small-molecular compounds, and a preparation method and application thereof. The pyrimidine compounds disclosed by the invention are represented as a general formula A. The method comprises the following steps: coupling iodochromone, which is used as a raw material, with various indolylboronic acids and azaindolylboronic acids, and condensing with amidine or guanidine compounds, thereby obtaining the pyrimidine compounds. The compounds have wide antitumor activity, and are hopeful to be prepared into new antitumor medicaments when being further optimized[General Formula A].
CN103288728A Naphthoyl amine derivative, and preparation method and application thereof The invention provides a naphthoyl amine derivative, and a preparation method and an application of the same. The naphthoyl amine derivative is N-(3- trifluoromethyl phenyl)-6-[(7- chloroquinoline-4-oxo) phenolic ether]-2- naphthoyl amine; the N-(3- trifluoromethyl phenyl)-6-[(7- chloroquinoline-4-oxo) phenolic ether]-2- naphthoyl amine can be used as protein kinase inhibitor and histone deacetylase inhibitor, and can be used for treating diseases caused by protein kinase dysregulation. The naphthoyl amine derivative can effectively treat the diseases caused by protein kinase dysregulation, and has the advantages of high bioavailability, obvious antitumor activity and low toxicity; moreover, the naphthoyl amine derivative is low in preparation reaction cost and higher in yield, the reaction process is simple and easy to control, so that the naphthoyl amine derivative is suitable for industrial production.
WO2007125105A3 Benzamide glucokinase activators The present invention relates to N-heteroaryl-benzamides, pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful in diseases or medical conditions mediated by glucokinase.
US20060235035 Novel methoxybenzamibe compounds for use in mch receptor related disorders Novel compounds of Formula (I) which modulate MCH activity are disclosed, in which A is a linker; Ar1 is an aryl or heteroaryl group; R1 is a lower alkoxy group; R2 is an R1 group or hydrogen, an OH or an NH2 group, Q together with the carbonyl forms an amide group, which is further substituted with an amine group; R5 is selected from hydrogen, halogen atoms, alkoxy groups, hydroxy, alkylamino groups, dialkylamino groups, hydroxylalkyl groups, carboxamido groups, acylamido groups, acyl groups, —CHO, nitrile, alkyl, alkenyl or alkynyl groups, —SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups such as —CH2CF3, —CF2CF3, —CF3, —OCF3, —SCF3; —SO2NH2, —SO2NHAlk, —SO2NAlk2, —SO2Alk; X is H, F, Cl, Br, I, —SCH3, —CF3, —OCF3, —SCF3, OCH3, or lower alkyl or alkenyl group; R8 is halogen atoms, alkyl, alkenyl or alkynyl groups, cycloalkyl groups, aryl groups, heteroaryl groups, heterocyclyl groups, alkylcycloalkyl groups, alkylaryl groups, alkylheterocyclyl groups, alkylheteroaryl groups, arylalkoxy groups, aryloxy groups, alkoxy groups, dialkylamino groups, —CONHAlk, —CONHAr, —CONAlk2, —NHCO-Alk, —NHCO—Ar, —CO-Alk, —CO—Ar, —SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups; or R8 is R6-Ar2—B—, in which B is a single bond or a connecting moiety; Ar2 is an Ar1 group; R6 is an R5 group; and which are useful in the treatment or prevention of e.g. obesity, depression, diabetes, bulimia etc.
CN102000074A Application of tetrahydroberberrubine in preparation of medicines for curing schizophrenia The invention relates to the field of natural medicines, in particular to an application of tetrahydroberberrubine in the preparation of medicines for curing schizophrenia. Tests of the influence of tetrahydroberberrubine on the amphetamine-induced high spontaneous activity, the antagonism of tetrahydroberberrubine to the apomorphine-induced climbing behavior, stupor and antagonism caused by tetrahydroberberrubine, and the like prove that tetrahydroberberrubine has higher activity of curing schizophrenia.
US20080085301 Method for transdermal administration of antimicrobial medications The present invention relates to methods and compositions for improved efficacy and delivery of time-dependent antimicrobial drug compositions to a patient. Transdermal dosage forms and methods for steady-state delivery of drug to produce and maintain a serum concentration of drug above the minimum inhibitory concentration or minimum microbicidal concentration are provided.
US7291624 Enzyme inhibitors as drugs for cardiovascular disorders, aids, alzheimers disease or urogenital disorders This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.
US8029811 Stabilized pharmaceutical product Use of an adsorbent and a sealed package (e.g. an overwrap) to protect a pharmaceutical product in a solid state in the presence of a reducing sugar.
EP1106176B1 Remedies for renal failure Remedies for renal failure containing a 4,8-inter-m-phenylene prostaglandin I2 derivative as the active ingredient; and a method for treating renal failure by using the same.
US7115585 Compositions for treating epithelial and retinal tissue diseases The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides.
CN103446087A Application of Incarviatone A in endometrial cancer treatment drug The invention discloses application of Incarviatone A in preparation of an endometrial cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Incarviatone A also has remarkable inhabiting effect on growth of human endometrial cancer cell strains ISK and RL95-2. Therefore, the Incarviatone A can be used for preparation of an anti-endometrial cancer drug and has good development and application prospect. The application of the Incarviatone A in the preparation of the endometrial cancer treatment drug is disclosed for the first time. Due to the fact that the fact that the skeleton type is a novel skeleton type, and the high endometrial cancer cell inhibiting activity of the Incarviatone A is previously unimagined.
CN102366444A Cooling patch and preparation method thereof The invention discloses a cooling patch and a preparation method thereof. The cooling patch is prepared from four materials of cooling oil, a surgical tape, gauze, and an anti-adhesion film. The preparation method comprises steps that: the gauze is stuck on the center of the surgical tape for later use; the cooling oil is mixed according to the requirement of a certain formula, and the cooling oil is well mixed and heated to a temperature of 38 to 40 DEG C; the molten liquid is injected onto the surgical tape with the gauze on the center; the surgical tape is cooled, and is sealed on the surface by using the anti-adhesion film. The cooling patch provides functions of fire purging, toxin removing, swelling subsiding and pain relieving. When the cooling patch is plastered on an afflicted part, the medicine permeates through the skin and directly reaches the focus of the disease. The curative effect is fast and direct. The cooling patch is safe and convenient, and causes no pain.
WO2006131653A1 Composition based on an avermectine and metronidazole in particular for treating rosacea The invention concerns a pharmaceutical, in particular dermatological, composition comprising, in a physiologically acceptable medium, at least one compound of the family of avermectines and metronidazole as well as its use for making a drug for treating skin conditions, in particular rosacea.
CN101987096A Melanogenesis inhibitor and skin-whitening agent The present invention provides a melanogenesis inhibitor and a skin-whitening agent. Particularly, the invention provides the melanogenesis inhibitor with a chemical formula (1) and the kin-whitening agent thereof.
CN101152181A Liquid composition containing loratadine and ambroxol hydrochloride The invention discloses a drug combination with loratadine and ambroxol hydrochloride as the active components and with the treating functions of allergy, relieving cough and expelling phlegm. The drug combination contains stabilizer, pH regulator, preservative, taste masking agent and metalion complexing agent, etc, and the existing forms of the product are syrups and oral liquid.
EP2629771A1 Use of pi3k inibitors for the treatment of obesity, steatosis and ageing The first aspect of the invention relates to a phosphoinositide 3-kinase inhibitor for use in the treatment or prevention of a disease or condition associated with the expression of peroxisome proliferator-activated receptor gamma coactivator 1-α (Pgd1α) and/or uncoupling protein 1 (Thermogenin/Ucp1 ) in brown adipocytes. The disease or condition may be positive energy imbalance-associated, for example, obesity, an obesity- associated disease or condition, steatosis and biological aging (performance aging). Another aspect of the invention provides the use of a phosphoinositide 3-kinase inhibitor for promoting weight loss in an individual.
US20120277263 Polymorphs of 1-cyclopropyl-7-([s,s])-2,8-diazadicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro -8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride and methods for the preparation thereof Two novel crystalline forms, designated form A and form B of the antibacterial agent 1-cyclopropyl-7-([S,S])-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride of formula, the preparation thereof, and their pharmaceutical compositions are described. These crystalline forms, which are characterized by greater stability and ease of preparation and of formulation, can be produced by industrially applicable methods which comprise the steps of: a) suspending 1-cyclopropyl-7-([S,S])-2,8-diazabicyclo-[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride in a solvent selected from an alcohol and a polyalcohol, b) heating the mixture under reflux, c) cooling, d) isolating the product which is separated, (form A) and, additionally, e) reslurrying the solid at reflux in a solvent selected from alcohols and polyols or mixtures thereof, in which the resulting mixture has an overall water content of between 2.5% and 0.01% by weight, f) isolating the product (form B).
US20100298391 Amide compounds and use thereof for plant disease control The present invention provides an amide compound represented by the formula (1): wherein R1 and R2 independently represent a hydrogen atom or a methyl group; and Cy1 represents a C3-C6 cycloalkyl group, said compound having excellent plant disease controlling effect.
CN103565790A Application of formononetin in cryptococcus neoformans The invention relates to application of formononetin in cryptococcus neoformans. The technical scheme of the invention is the application of formononetin in preparing medicaments for treating antifungal infected diseases, wherein the fungus is cryptococcus neoformans. The compound has an excellent antifungal activity on various superficial and deep funguses, has the advantages of high activity, low toxicity, broad antifungal spectrum and the like when being compared with an antifungal medicament in existing clinical application, and can be used for preparing antifungal medicaments.
CN102579341A Docetaxel solid lipid nanoparticle and preparation method thereof The invention belongs to the field of medicine preparation and particularly relates to a docetaxel solid lipid nanoparticle and a preparation method thereof. The docetaxel solid lipid nanoparticle consists of an effective curative dose of docetaxel, solid lipid materials, liquid lipid materials, an emulsifying agent, additives, long-circulating auxiliary materials and water for injection. The docetaxel solid lipid nanoparticle provided by the invention has the characteristics of stable docetaxel structure, phagocytosis prevention of an in-vivo reticuloendothelial system and active tumor targeting, and can be stably stored.
CN101415431A A method of treating cancer and/or cellular proliferative conditions and agents targeting hyaluronan anabolism useful for same The present invention is directed to compounds, agents, pharmaceutically active agents, medicaments, therapeutics, actives, drugs and the like which specifically target a portion of the HAS molecule which is accessible to the extracellular environment in a first form of a cell but which is not accessible to the extracellular environment in another form of or in a transformed cell form the same or related cell. In particular, the present invention provides compounds which target a portion of HAS which is accessible to the extracellular environment in malignant or inflammatory or proliferative cells but which portion is not accessible to the external environment in 'normal' cells. A 'normal' cell in this instance is a non-malignant, inflammatory or proliferative cell.
US20080045567 Therapeutic Agent for Hyperlipemia and Therapeutic Agent for Diabetes A therapeutic agent for hyperlipidemia, diabetes, or hypertriglyceridemia containing an HMG-COA reductase inhibitor and a carboxylic acid compound represented by the following formula (1) or a salt thereof as effective ingredients. The therapeutic agent of the present invention has excellent effects of lowering blood cholesterol and blood triglycerides and is particularly useful for treatment of type IIb and type IV hyperlipidemia and treatment of diabetes and also useful for treatment of hypertriglyceridemia.
CN101658640B Drug for treating cervical vertigo The invention relates to a drug for treating cervical vertigo, which is a capsule product prepared by the steps of evenly mixing earthworm after being processed with chrysanthemum, common selfheal fruit-spike, tall gastrodia tuber, gambir plant, simpleleaf shrub chastetree fruit, rehmanniae radix, radix salviae miltiorrhizae, indian buead, twotooth achyranthes root, inula flower, szechuan lovage rhizome, cassia seed, suberect spatholobus stem and liquoric root, blending with decocted nacre, red ochre and water, adding water for decoction, concentrating into a clear paste, drying, smashing, packaging into capsules and carrying out sterilization and disinfection. The drug has the effects of calming liver wind, clearing fire, dissipating phlegm, tonifying and nourishing qi and blood, lowering adverse qi, arresting vomiting, promoting blood circulation and dredging channels, is used for treating the cervical vertigo and has actual efficacy, and the clinical observation shows that the total effective rate is 100%.
US20090203768 Nucleic acid-containing complex A nucleic acid-containing complex, containing a nucleic acid and a biodegradable polymer, especially a positively-charged water-insoluble biodegradable polymer, is disclosed. The complex has excellent properties of sustainedly releasing a desired nucleic acid, especially DNA, to a site in need of a treatment. Since the complex can be taken up to phagocytes such as macrophages and delivered specifically to the target site, the function of the nucleic acid can be exhibited in a target site specific manner, and thus more specific gene therapy can be achieved. The complex has no adverse effects, such as occurrence of recombinants or toxicity which could be caused by using a virus vector such as adenovirus, or liposome. Thus, the complex is particularly preferable for the field of gene therapy. Furthermore, the complex enhances the biological effect of the nucleic acid introduced into the cells, allowing a gene therapy with a lower dose of nucleic acids.
EP1478382B1 Method for producing a powder inhalant containing a salt of the cgrp antagonist bibn4096 The invention relates to salts of the active substance 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine [BIBN4096] of formula (I). The invention also relates to the production of these salts, a method for producing a powder inhalant containing a salt of the active substance BIBN4096, and to the powder inhalants themselves that can be obtained by using said method.
US7622105 Conjugation product of a cytokine selected from tumor necrosis factor and interferon gamma and a ligand of CD13 receptor; antitumor agents Cytokine derivatives capable of homing the tumoral vessels and the antigen presenting cells and the use thereof as antitumoral agents.
WO2003070193A3 RNA interference mediated inhibition of HIV gene expression using short interfering nucleic acid (siNA) The present invention concerns methods and reagents useful in modulating human immunodeficiency virus (HIV) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against HIV gene expression and/or activity. The small nucleic acid molecules are useful in the treatment and diagnosis of HIV infection, AIDS, and any other disease or condition that responds to modulation of HIV expression or activity.
US7229969 Dipeptidyl peptidaseIV and alanyl-aminopeptidase inhibitors Combination of inhibitors of dipeptidyl peptidase IV (DP IV) and enzymes having the same substrate specificity (DP IV-analogous enzymatic activity) and inhibitors of alanyl aminopeptidase (aminopeptidase N, APN) and of enzymes having the same substrate specificity (APN-analogous enzymatic activity) for a more than additive to superadditive inhibition for the treatment of arteriosclerosis, for the treatment of allergic reactions of the type I according to the Gell and Coombs classification and for the treatment of dermatological diseases with follicular and epidermal hyperkeratoses and an enhanced proliferation of keratinocytes.
CN101293007A Pharmaceutical composition for bearing and rearing better children, preventing birth defect and improving anamnesis The invention relates to a pharmaceutical composition for prevention of birth defects and improvement of memory for healthy birth and sound care, the composition comprises largehead atractylodes rhizome, compound vitamin B, vitamin E and trace elements such as zinc, selenium, ferrum, chromium, copper, molybdenum, iodine and manganese, the composition is mainly applicable to pre-pregnancy women, pregnant women and lactating mothers and can effectively prevent the birth defects and improve the memory for the healthy birth and sound care; furthermore, the composition has the effects of health care and invigoration and does not have any side effects even in long-term application.
CN1843330A Slow release agent containing aminoglycosides antibiotic and its uses The invention relates to a slow-releasing agent of antibiotics containing aminoglycoside, comprising slow-releasing micro-sphere containing slow-releasing findings and aminoglycoside antibiotics, and special dissolvent containing suspending adjuvant agent such as sodium carboxymethyl cellulose with the adhesive degree being 100cp-3000cp (at 20-30 Deg. C). The slow-releasing findings comprises EVAc, polyphenyl, PLA, PLGA, decanedioic acid copolymer, albumen glue and gelatin; the slow-releasing micro-sphere can be produced to slow-releasing implanting agent and unguent agent. When the slow-releasing implanting agent and injection is placed or injected into bacteria, the medicine can be released slowly for more than 5-30 days, and toxicity is dramatically reduced at the same time when effective medicine concentration is got and maintained. The said slow-releasing agent is specially effective for chronic medullitis, bedsore, intractable ulcer on skin, diabetes femoral head necrosis and other abscessus, which are caused by Staphylococcus, Streptococcus, Streptococcus, acne Propionibacteriaceae, Enterobacter, Enterobacter, gonotoxin or parameningococcus.
US20120294846 Treatment of Pulmonary and Pleural Fibrosis Using HSP27 Inhibitors Reduction of HSP27 expression is in beneficial in the treatment of pleural and pulmonary fibrosis and in particular subpleural fibrosis and IPF. Pharmaceutical compositions for this purpose contain an inhibitor of HSP27 and a pharmaceutically acceptable carrier.
US20110076296 TLR3 Agonist Compositions The present invention relates generally to the fields of medicine. More specifically, the present invention relates to improved TLR3 agonists. The present invention provides novel dsRNA such as polyAU composition useful in the treatment of TLR3 related diseases, uses and preparations thereof.
US20100047360 Use Of Polyamines In The Treatment Of Psoriasis The present invention provides unbranched aliphatic polyamines for use in therapy, particularly for use in the treatment of psoriasis and compositions containing polyamines.
US20100298386 Compositions and methods for treating mastitis The present disclosure relates to compositions that are effective in controlling or in preventing mastitis in an animal. The disclosed compositions comprise a biocidal system, comprising a primary biocide and a preservative component; a nonionic surfactant having an HLB of from about 10 to about (20); an emollient system comprising an extradermal penetrating agent and an emollient base; a thickening agent; and an aqueous based carrier.
WO2011144777A1 Combination of n-acetylcysteine and lipoic acid for the treatment of a disease with axonal damage and concomitant oxidative lesions The present invention is a combination of N-acetylcysteine (NAC) and alpha lipoic acid (LA), or pharmaceutically acceptable salts thereof, for the prevention and/or treatment of a disease with axonal damage and concomitant oxidative lesions in a mammal, in particular X-linked adrenoleukodystrophy (X-ALD). The mouse model of X-ALD shows a late- onset neurological phenotype of the disease of locomotor deficit and axonal degeneration as predominant pathologies characteristic of the disease. The inventors have found that treatment of mouse models of X-ALD with these two active principles achieves reversal of oxidative stress and of the derived lesions to proteins of the spinal marrow as target organ of the disease, on the one hand, moreover however achieving prevention and reversal of axonal degeneration and furthermore correcting locomotor deficit presented by the mouse model of the disease, that is to say, the clinical symptomatology thereof.
US20090041756 121p1f1: a tissue specific protein highly expressed in various cancers A novel gene (designated 121P1F1) and its encoded protein are described. While 121P1F1 exhibits tissue specific expression in normal adult tissue, it is aberrantly expressed in multiple cancers including prostate, bladder, kidney, brain, bone, cervical, uterine, ovarian, breast, pancreatic, stomach, colon, rectal, leukocytic, liver and lung cancers. Consequently, 121P1F1 provides a diagnostic and/or therapeutic target for cancers, and the 121P1F1 gene or fragment thereof, or its encoded protein or a fragment thereof used to elicit an immune response.
WO2008114017A3 Compositions and methods relating to influenza infection The present invention provides a therapeutic composition for modulating inflammation in a subject in which reactive oxygen species is a causative agent, for treating, ameliorating or preventing an influenza infection in a subject and for treating, ameliorating or preventing pulmonary inflammation in a subject in which influenza is a causative agent, the therapeutic composition comprising a compound mimetic of superoxide dismutase. The invention also provides methods for modulating inflammation in a subject in which reactive oxygen species is a causative agent, for treating, ameliorating or preventing an influenza infection in a mammalian host, and for treating, ameliorating or preventing pulmonary inflammation in a subject in which influenza is a causative agent, the methods comprising administering the therapeutic composition to a subject.
US20120034240 Perlecan as a biomarker for renal dysfunction The application discloses PERLECAN as a new biomarker for renal dysfunction; methods for predicting, diagnosing, prognosticating and/or monitoring said dysfunction based on measuring said biomarker; and kits and devices for measuring said biomarker and/or performing said methods.
WO2008104993A1 Use of doxycycline in the treatment of idiopathic pulmonary fibrosis Use of doxycycline, a non specific matrix metalloproteinase inhibitor, for treatment of Idiopathic pulmonary fibrosis and a pharmaceutical composition comprising doxycycline or its congener in combination with another compound selected from the drug listed for treatment of IPF in a standard dose.
WO2009044930A1 Pharmaceutical composition for inhibiting the accumulation of amyloid-β protein Disclosed are: a pharmaceutical composition for inhibiting the accumulation of amyloid-β protein, which comprises a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; a method for inhibiting the accumulation of amyloid-β protein, which comprises the step of administering an effective amount of a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof to a mammal which is suspected to be diagnosed as being affected by a disease associated with amyloid-β protein; and others.
WO2011147311A1 Hydroxy propanediol derivatives, their preparative method, pharmaceutical compositions and use Compounds represented by formula (I), preparative method thereof and pharmaceutical compositions containing them and use thereof as immuno-regulation agents. The compounds can treat immunologic derangement, immunosuppression, hypoimmunity, rejection after organ transplantation, and autoimmune disease.
WO2011138398A1 Dosage regimen of diaryl sulfide derivatives A compound of formula (I) wherein X is O, S, SO or SO2; R1 is halogen, trihalomethyl, -OH, C1-7alkyl, C1-4alkoxy, trifluoromethoxy, phenoxy, cyclohexylmethyloxy, pyridylmethoxy, cinnamyloxy, naphthylmethoxy, phenoxymethyl, -CH2-OH, -CH2-CH2-OH, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, benzylthio, acetyl, nitro or cyano, or phenyl, phenylC1-4alkyl or phenyl-C1-4alkoxy each phenyl group thereof being optionally substituted by halogen, CF3, C1-4alkyl or C1-4alkoxy; R2 is H, halogen, trihalomethyl, C1-4alkoxy, C1-7alkyl, phenethyl or benzyloxy; R3 H, halogen, CF3, OH, C1-7alkyl, C1-4alkoxy, benzyloxy, phenyl or C1-4alkoxymethyl; each of R4 and R5, independently is H or a residue of formula (a) wherein each of R8 and R9, independently, is H or C1-4alkyl optionally substituted by halogen; and n is an integer from 1 to 4; or a pharmaceutically acceptable salt, hydrate, solvate, isomer or prodrug thereof; or a compound of formula (II) wherein R1a is halogen, trihalomethyl, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4alkylsulifinyl, C1-4alkyl-sulfonyl, aralkyl, optionally substituted phenoxy or aralkyloxy; R2a is H, halogen, trihalomethyl, C1-4alkyl, C1-4alkoxy, aralkyl or aralkyloxy; R3a is H, halogen, CF3, C1-4alkyl, C1-4alkoxy, C1-4alkylthio or benzyloxy; R4a is H, C1-4alkyl, phenyl, optionally substituted benzyl or benzoyl, or lower aliphatic C1-5acyl; R5a is H, monohalomethyl, C1-4alkyl, C1-4alkoxy-methyl, C1-4alkyl-thiomethyl, hydroxyethyl, hydroxypropyl, phenyl, aralkyl, C2-4alkenyl or -alkynyl; R6a is H or C1-4alkyl; R7a is H, C1-4alkyl or a residue of formula (a) as defined above, Xa is O, S, SO or SO2; and na is an integer of 1 to 4; or a pharmaceutically acceptable salt, hydrate, solvate, isomer or prodrug thereof, for use in a method of treatment, optionally of an autoimmune condition, wherein said compound of formula (I) or (II) is administered at a dosage lower than the standard daily dosage of said compound during the initial period of treatment and then is increased, optionally stepwise, up to the standard daily dosage of said compound.
WO2014100541A1 Substituted pyridine-2-carboxamide compounds as apoptosis signal-regulating kinase inhibitors The present invention relates to compounds of Formula (I) wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase ("ASKl") inhibitory activity, and are thus useful in the treatment of ASKl -mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
US20050202064 Administering an uronic acid or uronic acid derivative, a saccharide; anticarcinogenic A product obtained by heating at least one substance selected from the following (a), (b) and (c). (a) uronic acid or uronic acid derivative; (b) a saccharide compound containing uronic acid or a saccharide compound containing uronic acid derivative; and (c) a substance containing a saccharide compound containing uronic acid or a substance containing a saccharide compound containing uronic acid derivative; and food, beverage or a pharmaceutical agent which is characterized in containing the above-mentioned heat-treated product.
USRE39265 Heteroarylpiperidines, and their use as antipsychotics and analgetics Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
EP1503760A4 Camptothecin derivatives and polymeric conjugates thereof Polymeric conjugates of camptothecin derivatives having increased circulating half-lives are disclosed. In preferred aspects, the E ring lactone of the camptothecin derivatives is opened and funtionalzed to allow attachment of a polymer such as PEG in the 17-or 20-position thereof. A representative example of such compound is (I). Methods of preparing and using the same are also disclosed.
US20070129430 Agent for enhancing the production of collagen, their preparation and use The present invention has an object to provide an agent for enhancing collagen production and use thereof, and solves the object by establishing an agent for enhancing collagen production, which comprises as effective ingredients L-ascorbic acid or its derivative and a fatty acid or its derivative, and use thereof.
CN1961894A A novel compound pharmaceutical composition, preparation method and use thereof The invention relates to a method for preparing new compound drug, wherein it mainly comprises Cordyceps sinensis mycelium at 50-2000 deals or its extractive at 0.2-40 deals, and 10-500 deals of kuh-seng, while it also can contain 10-5000 deals of milk vetch root or the milk vetch root polysaccharide extractive at 0.1-100 deals, or the milk vetch root saponin at 0.1-100 deals. The invention can be made into oral or injection agent, with anti-cancer, antibiosis funtoins, etc.
CN1660101A Compound medicinal preparation of ligustrazine of phosphoric acids and xylitol, and preparation method A compound medicine for treating ischemic cerebrovascular diseases (cerebral ischemia, cerebral thrombosis and cerebral infarction) and the accompanied diabetes is prepared from ligustrazine and xylitol.
US20070225368 Therapy for Multiple Sclerosis The invention relates to a method of ameliorating multiple sclerosis and/or the symptoms of multiple sclerosis in a mammal, which comprises administering or having self administered to the mammal an effective amount of (a) cetyl myristate or (b) cetyl myristate and cetyl palmitate. In preferred embodiments the mode of administration is oral and both cetyl myristate and cetyl palmitate are administered.
EP1505072A2 Eplerenone crystalline form exhiniting enhanced dissolution rate A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
CN103087137A Glucocorticoid with sulfoalkyl group at position 21 The invention relates to glucocorticoid with a sulfoalkyl group at position 21 and provides a compound as represented by formula (I). In the formula (I), R1 is selected from the group consisting of aryl-, aralkyl-, cycloalkyl-, five-membered heterocyclic alkenyl-, six-membered heterocyclic alkenyl-, five-membered heteroaryl-, six-membered heteroaryl-, fused benzo-five-membered heterocyclic alkenyl- and fused benzo-five-membered heteroaryl-, R1 may be an unsubstituted group or a substituted group substituted by one to five independent substituents of an alkyl group, halogen, an alkyloxy group, -N(R2) or -CO2R2, R2 is independently selected from the group consisting of hydrogen, an alkyl group, an aryl group, a halogenated alkyl group and a heteroaryl group, R3 is selected from the group consisting of hydrogen and C1-C3 alkyl groups, R4 is selected from the group consisting of hydrogen, fluorine and bromine, R5 is selected from the group consisting of hydrogen, fluorine and C1-C3 alkyl groups, and A is a single bond or a double bond.
WO2009050218A1 Indazoles as glucocorticoid receptor ligands The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation and/or allergic conditions.
CN102600206A Nano composite skin disinfection lotion and preparation method thereof The invention discloses nano composite skin disinfection lotion and a preparation method thereof. The skin disinfection lotion comprises chlorhexidine acetate, zinc oxide, edetic acid, emulsifying agent and water. The emulsifying agent consists of vegetable oil, tri-n-butyl phosphate and triton x-100. The total volume ratio of the vegetable oil to the tri-butyl-phosphate to the triton x-100 is 2-8:1:1; the concentration of the chlorhexidine acetate is 0.5-3g/L, the concentration of the zinc oxide is 0.01-0.5g/L, the grain size is 50-100nm, and the concentration of the edetic acid is 0.01-0.2g/L. The nano composite skin disinfection lotion has the advantages of wide antibacterial spectrum of inorganic antibacterial agent, fine persistence and heat resistance, difficulty in drug resistance and the like, can achieve a prefect skin disinfection effect, and has an important application value.
CN1947725A Body wt.-reducing salt mud A salt mud for mud bath to lose weight and promoting blood circulation and metabolism is prepared from mineral salts (salt lake mud, mineral well salt and sea salt mud) (60-85 Wt%) and fresh water or sea water (15-40 Wt%) through dissolving.
WO2014113609A1 Stable indole-3-propionate salts of s-adenosyl-l-methionine Stable indole-3-propionic acid salts of S-adenosyl-L-methionine, or a pharmaceutically acceptable salt thereof, are disclosed, as well as pharmaceutical compositions comprising the indole-3-propionic acid salts, methods of using the indole-3-propionic acid salts and processes for making same.
EP1071671B1 Triazolones with a neuroprotective action The invention relates to the use of triazolones as medicaments, especially as medicaments with a neuroprotective action, to novel triazolones and to methods for producing them.
CN103341109A Natural drug extract and preparation method thereof The invention relates to a natural drug extract and a preparation method thereof. The natural drug extract consists of an extract prepared by decocting and concentrating amomum kravanh and clove in water, amomum kravanh ethyl acetate extract, clove ethanol extract and eugenol by a ratio of (1-4):(3-5):(2-6):(5-9). The composition has an extremely good treatment effect on diarrhea related with cancer chemotherapy and also has a synergism effect on cancer chemotherapy.
EP2391367A1 Nampt and vitamin b3 for treating or preventing diseases The present invention relates to the use of vitamin B3 and compounds derived therefrom as well as to nicotinamide phosphoribosyltransferase (NAMPT) and derivatives thereof as well as enhancers or inducers of NAMPT expression, NAMPT activity or NAMPT-mediated signalling for preventing or treating all types of cytopenia of the myeloid or lymphoid lineage. In a particular embodiment, the present invention relates to the use of the above referenced compounds for treating neutropenia, like severe congenital neutropenia or chemotherapy-induced febrile neutropenia or other congenital or acquired neutropenia. The invention also relates to the mobilisation of hematopoietic stem cells into peripheral blood. In another aspect, the present invention relates to pharmaceutical compositions containing as active ingredients vitamin B3 and metabolites thereof or NAMPT and modulators of the NAMPT activity, NAMPT expression or NAMPT mediated signalling in a combination with a therapeutically active or suboptimal amount of G-CSF.
EP1701943A1 5-ht2 receptors modulators, their pharmaceutical compositions and their use for the treatment of cardiovascular and muscle diseases The present invention provides certain compounds, pharmaceutical formulations thereof, and methods for the treatment of conditions mediated by 5-HT2 receptors. These compounds provide for modulation of the signals mediated by 5-HT2 receptors, specifically those receptors in the cardiovascular system. Thus, these compounds may be used alone or in conjunction with other drugs to treat cardiovascular diseases such as, but not limited to, muscle atrophy, cardiac hypertrophy, heart failure, and primary pulmonary hypertension.
US20100172991 Extended Release Formulation and Methods of Treating Adrenergic Dysregulation A composition and method of treating adrenergic dysregulation by administering the composition is disclosed, wherein the composition comprises a α2-adrenergic receptor agonist; a pharmaceutically acceptable hydrophilic matrix and a release-retardant of a metal alkyl sulfate. In embodiments, the composition provides a sustained release of the agonist, wherein after administration of the composition no more than once about every 12 hours (e.g., no more than once about every 24 hours) to a subject having a steady state plasma concentration of the α2-adrenergic receptor agonist, the agonist's plasma concentration peak-to-trough ratio is no greater than about 1.9.
WO2011143163A1 Substituted n-phenyl spirolactam bipyrrolidines, preparation and therapeutic use thereof The present invention discloses and claims a series of substituted N-phenyl spirolactam bipyrrolidines of formula (I). (Formula (I)) Wherein R1, R2, R3, R4, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl spirolactam bipyrrolidines of formula (I) and intermediates therefor.
US20100056505 Substituted Pyrazalones The invention is related to compounds of formula (I) as antagonists of the TGFβ family type I receptors, Alk5 and/or AIk 4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such as fibrosis (e.g., renal fibrosis, pulmonary fibrosis, and hepatic fibrosis), progressive cancers, or other diseases for which reduction of TGFβ family signaling activity is desirable.
WO2006117220A3 Method of administering a cationic liposomal preparation comprising paclitaxel The present invention relates to the use of a cationic liposomal preparation comprising at least one cationic lipid from about 30 mol% to about 99.9 mole%, paclitaxel in an amount of at least about 0.1 mol% and at least one neutral and/or anionic lipid from about 0 mole% to about 70 mole% for the manufacture of a pharmaceutical composition for administration (i) once in a week, (ii) twice in a week or (iii) a combination of (i) and (ii), wherein the monthly dose is about 0.1 mg/kg bw to about 20 mg/kg bw.
US20080254147 Composition comprising clay as the active ingredient is administered to stop bleeding wound; type A or B hemophilia or von Willebrand disease In a method of clotting blood in which the blood exhibits a reduced tendency to clot and may be from a person undergoing an anticoagulant therapy or having type A or B hemophilia or von Willebrand disease, a therapeutically effective amount of a composition comprising clay as the active ingredient is administered to a wound from which the blood emanates. Upon contacting the blood, this clay, which may be kaolin, bentonite, or any type of layered clay, causes the blood to clot. In a method of arresting blood flowing from a wound, a therapeutically effective amount of a composition comprising clay as the active ingredient is administered to the bleeding wound. In this method, the blood has a reduced tendency to clot and may be from a person undergoing an anticoagulant therapy or having at least one of hemophilia A or B or von Willebrand disease.
US20110053929 Imidazo-, pyrazolopyrazines and imidazotriazines and their use The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias.
CN102920920A Efficient powerful rhizoma gastrodiae and cortex eucommiae soft capsule or preparation The invention discloses an efficient powerful rhizoma gastrodiae and cortex eucommiae soft capsule or preparation which is characterized by consisting of the following raw materials in parts by weight: 35-40 parts of rhizoma gastrodiae, 37-43 parts of cortex eucommiae, 5-7 parts of angelica, 5-7 parts of radix scrophulariae, 5-7 parts of rhizoma et radix notopterygii, 2-4 parts of radix angelicae pubescentis, 0.5-1 part of radix aconiti agrestis, 0.5-1 part of radix aconiti lateralis preparata, 4-6 parts of mistletoe, 10-13 parts of semen citri reticulatae, 8-12 parts of raddle and 8-12 parts of poria. According to the invention, by changing the raw materials and the component amount based on the prior art, the efficient powerful rhizoma gastrodiae and cortex eucommiae soft capsule or preparation disclosed by the invention realizes an obvious treatment effect on pain, blood stasis, cerebral ischemia and the like, and also can adjust the TH1 and TH2 balance, obviously enhance the immunity and reduce the macrophage activity.
EP0804194B1 Use of retinoic acid receptor-agonists or ap-1 antagonists for the manufacture of a medicament for preventing proliferation of retinal pigment epithelium Proliferation of retinal pigment epithelium following surgery or trauma or resulting in ocular diseases associated with choroidal neovascularization, such as age related macular degeneration and histoplasmosis syndrome, is prevented by contacting retinal pigment epithelium cells with a therapeutic amount of a retinoic acid receptor (RAR) agonist, preferably one with specific activity for retinoic acid receptors. Preferably the RAR agonist is also a potent antagonist of AP1-dependent gene expression. Alternatively, the proliferation of retinal pigment epithelium is ameliorated with a therapeutic amount of an AP-1 antagonist, alone or in combination with an RAR agonist. The drug can be administered by bolus injection into the vitreous cavity using a dosage from about 50 to 150 mu g, or by slow release from liposomes or an oil tamponade injected into the vitreous cavity. Formulations for preventing proliferation of retinal pigment epithelium are also provided.
WO2009125808A1 Aminocyclohexyl derivative It has been demanded to develop a substance which has a potent and wide-spectrum anti-bacterial activity against gram-positive bacteria, gram-negative bacteria and resistant bacteria thereof and is highly safe. Under these circumstances, extensive studies have been made, and it is now found that a compound represented by formula (I) or a salt thereof has a potent and wide-spectrum antibacterial activity against gram-positive bacteria and gram-negative bacteria and also has high safety at a level suitable for use as an antibacterial agent or a prophylactic or therapeutic agent for infectious diseases. Thus, disclosed is a compound represented by formula (I), a pharmacologically acceptable salt thereof, or a hydrate of the compound or the salt.
US20110201655 Pharmaceutical composition improving intestinal absorption An object of the present invention is to provide a pharmaceutical composition that improves intestinal absorption of a compound having a structure represented by the general formula [1]. The composition containing a compound represented by the general formula [1] or a salt thereof and (b) a lipophilic substance improves intestinal absorption of the compound. In the formula, A represents —(NR4)—, —(CR5R6)— or the like; B represents an alkylene group or an alkenylene group; R1 represents an alkyl group, an alkenyl group or the like; R2 represents an adamantylalkyl group or the like; R3 represents an unsaturated heterocyclic ring; R4, R5 and R6 each represent a hydrogen atom or the like; and X represents an oxygen atom or the like.
CN101914552A S. agalactiae antigens i + ii The present invention discloses isolated nucleic acid molecules encoding a hyperimmune serum reactive antigen or a fragment thereof as well as hyperimmune serum reactive antigens or fragments thereof from S. agalactiae, methods for isolating such antigens and specific uses thereof.
WO2011071716A1 Heterocyclic compounds containing an indole core Disclosed are novel compounds which inhibit RSK, methods of making such compounds and pharmaceutical compositions comprising such compounds. Also disclosed are methods of treating RSK2 regulated disorders using compounds of the invention.
CN103751155A Ornidazole oral cataplasm The invention provides an ornidazole oral cataplasm having biological adhesion. The ornidazole oral cataplasm comprises ornidazole and a water-soluble matrix having biological adhesion. The water-soluble matrix having biological adhesion comprises carbopol, lactose, low-substituted hydroxy propyl cellulose and carboxymethylcellulose sodium. A preparation method of the ornidazole oral cataplasm having biological adhesion comprises the following steps of respectively screening prescribed amounts of ornidazole, lactose, low-substituted hydroxy propyl cellulose and carboxymethylcellulose sodium by a sieve of 80 meshes, carrying out full mixing to obtain a uniform mixture, adding ethanol having the content of 70% into the mixture, carrying out granulation, carrying out drying, carrying out granule size stabilization by a sieve of 30 meshes, adding carbopol, magnesium stearate and talcum powder screened by a sieve of 100 meshes into the granules, carrying out full mixing to obtain a uniform mixture and carrying out tabletting. The ornidazole oral cataplasm is used for treating oral ulcer, can be bonded to the surface of a mucous membrane, prolongs drug release time and improves curative effects.
CA2198630C Acetaminophen sustained-release formulation An orally administrable sustained-release dosage form includes particles of an active pharmaceutical ingredient which is coated with a polymeric material that is water-insoluble, but water-permeable and water-swellable, so that the sustained-release dosage form provides controlled release which is independent of certain variable physiological factors such as pH. In accordance with one aspect of the invention, the active pharmaceutical ingredient is acetaminophen and the coated acetaminophen particles are combined with uncoated acetaminophen particles to provide a combination immediate-release/sustained-release dosage form. In accordance with another aspect of the invention, the active pharmaceutical ingredient is coated with a methacrylate ester copolymer, and the coated particles are combined with uncoated particles of an active pharmaceutical ingredient to provide a combination immediate-release/sustained-release dosage form, wherein the sustained-release component provides a release rate which is substantially independent of physiological factors such as pH. The final orally administrable dosage form can appear as compressed tablets, capsules or pouches.
EP2478900A1 Monohydrate creatins intended for regulating the hormone secretions and infertility of the cycle, in vitro fertilisation and artificial insemination Composition (I) comprises creatine monohydrate or citrate salts in the form of micronized powder, where the creatine monohydrate salts are present either alone or in combination with excipient. - ACTIVITY : Endocrine-Gen.; Antiinfertility. - MECHANISM OF ACTION : None given.
CN103755673A Compound and method for treating estrogen receptor-related diseases The present invention relates to a compound and a method for treating estrogen receptor-related diseases. The present invention relates to the compound represented by the following formula (I). The compound or medicinal salt thereof is used for preventing or treating diseases involving abnormal cell proliferation related to ER-alpha in a main body.
WO2013138568A1 Liver x reception modulators Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
US20100317620 N-PHENYLIMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE COMPOUNDS, PREPARATION AND THERAPEUTIC USE THEREOF Compounds of formula (I): in which X, R1, R2, R3, and R4 are as defined in the disclosure, or an acid addition salt thereof; and therapeutic uses thereof.
EP2749295A1 Radiopharmaceutical and pharmaceutical kit A radiopharmaceutical comprising a particular radioactive dithiosemicarbazone copper complex, wherein the radiopharmaceutical is used for combined administration with a chelating agent, and wherein the chelating agent comprises a multidentate ligand having a maximum dentate number of 2 or more to 4 or less.
US20050124609 Orally administering to a patient a methylol transfer agent; e.g., an oral dose of about 100-1000 mg. of taurolidine, taurultam or mixtures; ulcerative colitis; Crohn's disease; reduces side effects when administered with other drugs; synergistic; bactericides; endotoxins; antiinflammatory agents Patients suffering from inflammatory bowel disease such as Crohn's disease or ulcerative colitis are treated either orally or intravenously with methylol transfer agents, such as taurolidine and/or taurultam. These agents can be used in combination with other drugs thereby allowing the use of smaller amounts of the other drugs and limiting unwanted side effects.
CN101899056A Prasugrel hydrobromide polymorph and preparation method thereof The invention mainly relates to prasugrel hydrobromide polymorph and a preparation method thereof.
CA2631071A1 Inhibition of calpain reduces allergic inflammation The present invention provides for the use of a calpain inhibitor for the treatment of allergy diseases, inflammatory diseases and autoimmune diseases. In particular, it has been found that inhibition of calpain within mast cells decreases the release of chemical mediators into the surrounding environment, resulting in a decreased local inflammatory response. The present invention also provides for a method of decreasing IgE-dependent mast cell degranulation, mast cell mediator release and cytokine production in mast cells, comprising the step of administering to the mast cells an effective amount of a calpain inhibitor.
CN1771920A Oral disintegrated sertraline tablet and its prepn The present invention belongs to the field of medicine, and is especially one kind of oral disintegrated tablet of sertraline as depression treating medicine and its preparation process. The oral disintegrated tablet of sertraline includes sertraline as the effective medicine component and excipient mixture comprising disintegrating agent, stuffing, soluble polyol and penetrant. Specifically, the oral disintegrated tablet of sertraline contains sertraline 20-50 wt%, disintegrating agent 5-15 wt%, stuffing 10-30 wt%, soluble polyol 30-60 wt% and penetrant 1-5 wt%. Compared with other oral preparation forms, the present invention has wide covering of disintegrated medicine on gastrointestinal tract mucous membrane resulting in fast acting, no first pass effect, high bioavailability, less stimulation to gastrointestinal tract and easy taking.
CN103539791A Modulators of the GPR119 receptor and the treatment of disorders related thereto The present invention relates to the GPR119 receptor agonists:3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-dimethylbenzamide; -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
CN103006590A Dispersible tablet for chronic ulcerative colitis and preparation method thereof The invention discloses a dispersible tablet for chronic ulcerative colitis and a preparation method thereof. The dispersible tablet for chronic ulcerative colitis comprises the following material components in parts by weight: 50 parts of salazosulfapyridine, 10 parts of sodium carboxymethyl starch, 13.2 parts of polyvinyl polypyrrolidone, 24 parts of microcrystalline cellulose, 0.5 part of magnesium stearate, 0.5 part of aerosol and 50 parts of alcohol. The anti-inflammatory drug for treating ulcerative colitis disclosed by the invention has the advantages of small dosage, convenience in taking, fast absorption, high bioavailability, convenience in carrying, accurate ration, stable quality and the like to the ulcerative colitis and the non-specific ulcerative colitis in comparison with other relevant products.
CN103371977A Tebipenem ester particles and preparation method thereof The invention relates to tebipenem ester particles and a preparation method thereof. The tebipenem ester particles are prepared by selecting the appropriate variety and usage amount of auxiliary materials and using an appropriate preparation method. The tebipenem ester particles provided by the invention are characterized in that the tebipenem ester particles comprise main drug particles, a main drug particle coating solution and taste modifying particles, wherein the main drug particles comprise 65-130 parts by weight of tebipenem ester, 150-300 parts by weight of microcrystalline cellulose, 100-200 parts by weight of cane sugar, 10-20 parts by weight of aspartame, 15-30 parts by weight of hydroxypropyl methylcellulose (E50) and a right amount of 90% alcohol; the main drug particle coating solution comprises 80-160 parts by weight of polypropylene resin IV and a right amount of 90% alcohol; and the taste modifying particles comprise 50-100 parts by weight of cane sugar, 15-30 parts by weight of microcrystalline cellulose, 10-20 parts by weight of aspartame, 5-10 parts by weight of hydroxypropyl methylcellulose, a right amount of strawberry essence and a right amount of 90% alcohol. The tebipenem ester particles provided by the invention have good mouth feel, can effectively cover the bitter of tebipenem ester and are particularly suitable for being taken by children. The preparation method is simple. The preparation has good stability and is low in cost and practicable for industrial production.
WO2008003242A1 Method and ophthalmic formulation for eye protection or treatment An ophthalmic composition for artificial tears useful for treating dry eye symptoms or for general eye protection is provided. The composition includes a physiologically balanced salt solution and one or more anti-oxidative ingredients which collectively confer on said ophthalmic composition a total antioxidant capacity as a FRAP value of greater than 100μmol/l, preferably greater than 150μmol/l. The composition also has peak UV absorption in the range of 200-350nm. Suitable anti-oxidative ingredient includes ascorbate, urate, cysteine, glutathione, tyrosine, lactoferrin, transferrin, albumin, caeruloplasmin and lacrimal gland peroxidase.
WO2013016193A2 Activators of class i histone deacetlyases (hdacs) and uses thereof The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (amyotrophic lateral sclerosis), traumatic brain injury, ischemic brain injury, stroke, frontal temporal dementia, Pick' s disease, corticobasal degeneration, supra cerebral palsy, prion diseases (e.g., Creutzfeldt- Jakob disease, Gerstmann-Straussler-Scheinker syndrome, Fatal Familial Insomnia, and Kuru), Nieman Pick type C, spinal cerebellar ataxia, spinal muscular dystrophy, ataxia telangiectasia, hippocampal sclerosis, Cockayne syndrome, Werner syndrome, xeroderma pigmentosaum, and Bloom syndrome. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).
CN1810237A Slow-released ambroxol salt tablet and its prepn process The slow-released ambroxol salt tablet consists of ambroxol salt 10-60 wt%, retarder 10-50 wt%, and medicinal supplementary material. It has specific extracorporeal releasing degree in water, buffering liquid or simulated physiological environment. The slow-released ambroxol salt tablet has simple production apparatus, easy control of the medicine releasing speed, less influence of physiological factors, pH value, movement, etc of intestinal tract on the medicine releasing speed, less disintegrating possibility, taking safety, less toxic side effect and high bioavailability, and can meet the requirement of different types of patients.
EP2004187A1 Dietary supplement for healing or regressing symptoms of gastroesophageal reflux disease, gastritis and ulcers The current invention presents a dietary supplement obtained from a mixture of melatonin, vitamins and aminoacids for healing or regressing symptoms of gastroesophageal reflux disease (such as heartburn, regurgitation, dysphagia, coughing, hoarseness, chest pain and odynophagia), gastritis and several types of ulcerations.
CN101220035B A kind of alkaloid, method for preparing the same and application in antineoplastic or antimicrobial aspects The invention relates to the technical field of organic compounds, in particular to an alkaloid, a preparation method thereof and the application of the compound in anti-tumor and antisepsis. A general formula of the alkaloid is indicated by a formula (I), and the preparation method is that the alkaloid can be acquired by reaction between analogues of Mansonone and ammonia, fatty primary amine, hydroxylamine or diamine. The alkaloid of the invention has relatively good antibacterial and anti-tumor activity, and in the preparation method, the synthetic method of the ammonia with Alpha CH2 and quinine is not high yield but is simple in steps. But in the prior art, such a complex heterocyclic system is difficult to be constructed in simple ways under normal circumstances; therefore, the preparation method of the invention is significant in constructing the alkaloid with complex ring systems.
WO2009043784A1 Cyclopropyl aryl amide derivatives and uses thereof Compounds of the formula (I) wherein Ar1, Ar2, R1 and R2 are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.
WO2008084864A1 Capsaicin receptor activator and apparatus for spraying the same [PROBLEMS] To provide a capsaicin receptor agonist (activator) having the same various physiological activities as those of capsaicin and has no pungency, and to provide a capsaicin receptor activator which is readily available, is highly safe, shows no adverse side effect even when ingested for a long period, and has high efficacy. [MEANS FOR SOLVING PROBLEMS] Disclosed is a capsaicin receptor activator comprising, as an active ingredient, a monoacylglycerol having a saturated or unsaturated fatty acid having 2 to 22 carbon atoms as a constituent fatty acid.
EP0866713B1 Administration media for analgesic, anti-inflammatory and anti-pyretic drugs containing nitrous oxide and pharmaceutical compositions containing such media and drugs Administration mediums comprising solutions of nitrous oxide in water, alcohols, ethers or oils, and optionally including essential fatty acids or C1-C6 alkyl esters thereof enhance the action of analgesic, anti-inflammatory and anti-pyretic drugs. The drugs may be combined with the medium into a pharmaceutical composition or may be taken orally by swallowing the drug with the aid of the medium.
US20140112904 Method for enhancing the cleavage activity of i-crei derived meganucleases A method for enhancing the cleavage activity of an I-CreI derived meganuclease, comprising the site-specific mutation of at least one amino acid residue which is selected in the group consisting of: the glycine at position 19, the phenylalanine at position 54, the phenylalanine at position 87, the serine at position 79, the valine at position 105 and the isoleucine at position 132 of I-CreI, and its application for the manufacturing of meganuclease cleaving a DNA target of interest, for use in genome therapy (treatment of genetic diseases) and genome engineering (making of transgenic animals, transgenic plants and recombinant cell lines).
CN103356693A Compound low-molecular heparin sodium liposome gel and preparation method and application thereof The invention belongs to the technical field of medicines and relates to a compound low-molecular heparin sodium liposome gel and a preparation method and application thereof. The compound low-molecular heparin sodium liposome gel comprises low-molecular heparin sodium, asiaticoside, lipid components, a membrane softening agent and gel matrix components, wherein the low-molecular heparin sodium and asiaticoside are pharmacological active ingredients, and based on the total gel of 100g, the content of the low-molecular heparin sodium is 5000-35000IU, and the content of the asiaticoside is 0.1-2.5g. The preparation method comprises the following steps of: (1) preparing a compound low-molecular heparin sodium liposome by employing an ethanol injection-ultrasonic method or ethanol injection-high pressure homogenizer method; (2) preparing a blank gel; (3) adding the compound low-molecular heparin sodium liposome into the blank gel, uniformly stirring, and obtaining the compound low-molecular heparin sodium liposome gel. The gel is mainly used for treating skin injury and scar.
US7785626 proton pump inhibitor and histamine H2 receptor antagonist; sustained release; for treatment of conditions associated with an excessive secretion of gastric acid; provides a suitable combination of a rapid onset and a long-lasting duration of the effect An oral pharmaceutical dosage form comprises pharmacologically effective amounts of an acid-susceptible proton pump inhibitor and an H2 receptor antagonist in combination with at least on pharmacologically acceptable excipient which causes a delayed release and/or an extended release of the proton pump inhibitor. The H2 receptor antagonist is included in the dosage form in such a way that it is rapidly released after administration. This dosage form is suitable for the treatment of conditions associated with an excessive secretion of gastric acid and provides a suitable combination of a rapid onset and a long-lasting duration of the effect. The invention also relates to a method for manufacturing such a dosage form and to a method for the treatment of conditions associated with the secretion of gastric acid.
CN1927177A Anticancer drug composition loading both platinum compound and tetrazole violet Disclosed is an anti-cancer pharmaceutical composition carrying both platinum-group compounds and tetrazole lonone, characterized in that the pharmaceutical composition is in the form of slow release injection or slow release implanting agent, the slow release injection comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents include the combination of tetrazole lonone or its analogues with cisplatin, Carboplatin, Eptaplatin, Enloplatin, Lobaplatin, Nedaplatin, Ormaplatin, Oxaliplatin, the slow release auxiliary materials include polylactic acid and its copolymer, polyethylene glycol, PLA-COOH copolymer, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid), Polifeprosan, poly(lactic acid), biological compatible EVAc, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose. The slow release agent can be injected or placed in or around tumor, or used in combination with non-operative treatment methods such as chemotherapy.
CN102342958A Vinegar egg liquid for treating neurodermatitis The invention discloses a treatment method for treating neurodermatitis. The method is characterized in that: eight fresh duck eggs are immersed in 750g of vinegar for one month, an egg white is coated on an affected part, and simultaneously one duck egg is orally taken each day.
CN1732963A Novel use of ginsenoside Rg1 The invention relates to a novel use of ginsenoside Rg1, especially the use in preventing or treating male sexual dysfunction such as ejection dysfunction.
CN103271966A Composition for controlling porcine respiratory disease complex and application thereof The invention discloses a composition for controlling porcine respiratory disease complex and an application thereof. The composition comprises the following components: an echinacea purpurea herb extract product, nano-zinc oxide, Mycobacterium phlei, farrerol, deoxyglucose and astragalus polysaccharide. The composition is used as a feed additive to be applied for controlling porcine respiratory disease complex. By the adoption of the composition provided by the invention, the vast majority of disease causes which trigger porcine respiratory disease complex can be effectively inhibited and killed, various clinical symptoms can be controlled, course of the disease is shortened, death and culling rate is minimized, and growth speed of pigs is raised.
US7074784 Medicaments against viral diseases Novel dihydropyrimidines and combinations thereof with other antiviral agents, suitable for combating HBV infections.
CN101550173A 4-(4-beta-D-allopyranosid-phenyl)-2-aryl-5-nitrilyl-6-methoxyl pyridine and preparation method and application thereof The invention discloses a helicldum derivative 4-(4-beta-D-allopyranosid-phenyl)-2-aryl-5-nitrilyl-6-methoxyl pyridine, and the structure is represented by the right formula; in the structure, R is H, or alkyl, or ether, or halogen, or nitryl, or amino; the compound has stronger calmed and somnific functions than helicidum, and the effective time is longer than helicidum. The preparation method includes the following steps: (1) synthesizing E-4-beta-D-allopyranosid-phenylvinyl-4-substituted phenyl ketone; (2) synthesizing 4-(4-beta-D-allopyranosid-phenyl)-2-aryl-5-nitrilyl-6-methoxyl pyridine.
CN101935334A Berberine glycyrrhetinic acid enantiomeric salts and preparation method and application thereof The invention discloses novel organic berberine glycyrrhetinic acid enantiomeric salts used for medicines and a production method and application thereof. The chemical name of the organic berberine glycyrrhetinic acid enantiomeric salts is: 5,6-dihydrogen-9,10-dimethoxybenzo[g]-1,3-benzodioxolane[5,6-a]quinolizidine.18a(beta),3beta-hydroxyl-11-oxooleanane-12-olefine-30-formate. The production method comprises the following steps of: respectively dissolving berberine and a glycyrrhetinic acid enantiomer in 80 percent ethanol according to a medicament eutecticum principle, mixing the two liquids, stirring for 2 hours, removing the ethanol under reduced pressure, and treating by using ethyl acetate to prepare the berberine glycyrrhetinic acid enantiomeric salts. The organic salts with dual parent nuclei have positive practical significance for resisting diseases such as tumors, diabetes, chronic inflammatory diseases such as rheumatoid arthritis, hepatitis, Alzheimer disease and the like of human and developing medicines.
US20080269248 Tartrate and Malate Salts of Trans-1-((1R,3S)-6-Chloro-3-Phenylindan-1-Yl)-3,3-Dimethylpiperazine A tartrate and malate salt of trans-1-(6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine, in particular for medical use, pharmaceutical formulations thereof, including for treatment of schizophrenia or other diseases involving psychotic symptoms.
US20080260845 Multiple active drug resin conjugate A combination pharmaceutical preparation including two different active drugs of the same ionic charge conjugated with a single resin particle, without one significantly displacing the other, and without retarding the initial availability of either active. Also, methods for the manufacture of a multiple active drug-resin conjugate, and for the in vivo release of a combination of pharmaceutically active drugs from a multiple active drug-resin conjugate.
EP1448220B1 Pharmaceutical composition comprising an antiphlogistic agent and lactalbuminhydrolysate and the use thereof The invention relates to pharmaceutical agents based on antiphlogistic active substances and to the use thereof in the treatment of diseases in the rheumatic sphere. The agents contain lactalbumin hydrolysate or a fraction thereof. Said hydrolysate allows smaller doses of the antiphlogistic agents to be administered than is conventionally required, to achieve a specific antiphlogistic effect.
CN101926816A Intravenous injection of nelarabine and preparation method thereof The invention provides an intravenous injection of nelarabine and a preparation method thereof. The injection of the invention contains propanediol, has high thermal stability and is used for treating refractory or recurrent acute lymphoblastic leukemia.
CN1651085A Compound aspirin tading kind medicinal preparation and its application A compound aspirin-tatin medicnie contains proportionally aspirin, the medicine in tatin kind, hypolipemic medicine, dihydroxyaluminium aminoacetate, heavy magnesium carbonate or magnesium aluminate carbonate, skeleton and medical auxiliary. Its application is also disclosed.
CN101380324A Pharmaceutical composition containing lacidipine and atorvastatin and preparation method and use thereof The invention discloses a pharmaceutical composite containing lacidipine and atorvastatin, a preparation method and the application thereof, and relates to a pharmaceutical composite for treating cardiovascular diseases such as hypertension, hyperlipemia and the like, and a preparation method and the application thereof. The pharmaceutical composite is made from 1-10 parts of the lacidipine and 1-10 parts of the atorvastatin or a derivative thereof according to the parts by weight. The preparation method of the pharmaceutical composite comprises the following steps: the lacidipine, the atorvastatin or the derivative thereof and pharmaceutic adjuvants are respectively crushed into powder, sieved by a 60-100 mesh sieve, added with 5-20% slurry to prepare soft wood which is made into 20-50 mesh pelletization; the pelletization is dried at the temperature of 50-90 DEG C, added with a proper amount of a lubricant and then evenly mixed to prepare a corresponding preparation. The pharmaceutical composite has the advantages of lowering the blood pressure and the blood fat simultaneously, improving the effect of lowering the blood pressure by independently using the lacidipine, and stopping the shortage caused by independent use of antihypertensives and antihyperlipidemic.
WO2014012034A1 Fused benzazepines for treatment of tourette's syndrome The present invention encompasses methods of treating a subject who has been diagnosed as having a tic disorder or a movement disorder. The tic disorder can be Tourette's Syndrome, and the methods can include the steps of: (a) identifying a subject in need of treatment; and (b) administering to the subject a therapeutically effective amount of a composition comprising a D1/D5 receptor antagonist, a D1/D5 receptor partial agonist, or a mixture thereof. For example, the D1/D5 receptor antagonist can be ecopipam or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, structural analog, metabolite, or polymorph thereof.
US20080160033 Novel Screening Method By using a G protein-coupled receptor protein comprising the same or substantially the same as the amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 3 or SEQ ID NO: 8, or a salt thereof, and a fatty acid, a compound or its salt that changes the binding property of the receptor protein or a salt thereof to the fatty acid can be efficiently screened.
DE102005019094A1 New aza-heterocyclic compounds are tyrosine kinase inhibitor useful to prevent and/or treat cancer, tumor growth, tumor angiogenesis, arteriosclerosis, diabetic retinopathy and inflammation diseases Aza-heterocyclic compounds (I) and their salts, derivatives, solvates and/or stereoisomers are new. Aza-heterocyclic compounds of formula (I) and their salts, derivatives, solvates and/or stereoisomers are new. R1>H, A, Ar, Ar-A or A-Ar; A : 1-14C (cyclo)alkyl, where 1-2 CH2-groups are optionally replaced by O, S, NH, N-A, CONH, NHCO and/or -CH=CH-, and/or 1-7 H-atoms are optionally replaced by Hal; and where 1-2 CH3-groups are optionally replaced by NH2, NAH, NA2 or CN; Ar : mono- or bicyclic (hetero)aromatic group with 5-10 ring members and optionally 1-4 N, O and/or S-atoms (optionally mono-, di- or trisubstituted with carbonyl oxygen, Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 and/or S(O)2A); Hal : F, Cl, Br or I; X : CH or N, where 1 X group is N and 2 X groups are CH; Y1>CH2 or a saturated bond; Z : CH or N, where 0-2 (preferably 0 or 1) Z groups are NH; R-2a, R-2b, R-2c : H, Hal, OH, CN, NH2, 1-4C alkyl, where CH2 groups are optionally replaced by O, S, NH, N-A, CONH, NHCO and/or -CH=CH-, and/or 1-4 H-atoms are optionally replaced by Hal; and where a CH3-group is optionally replaced by NH2, NAH, NA2 or CN; R3>H or A; g : 0-2; and bond marked with asterisk : single or double bond. Independent claims are included for: (1) a method for the preparation of (I); (2) a medicament comprising (I), carrier- and/or auxiliary- materials; and (3) a kit comprising (I) and the medicament. [Image] - ACTIVITY : Cytostatic; Antiangiogenic; Antiarteriosclerotic; Antidiabetic; Ophthalmological; Antiinflammatory. - MECHANISM OF ACTION : Tyrosine kinase inhibitor; Insulin like growth factor-1 receptor inhibitor. The insulin like growth factor-1 receptor inhibiting activity of (I) was tested using biological assays. The results showed that (I) exhibited a median inhibitory concentration (IC50) value of 0.76 mu M.
DE102004010254A1 New 4-heterocyclyl-1-acyl-piperidine derivatives, useful e.g. for treating headache, diabetes and cardiovascular disease, are antagonists of calcitonin-gene related peptide 4-heterocyclyl-1-acyl-piperidine derivatives (I), their tautomers, diastereomers, enantiomers, hydrates and/or (hydrated) salts are new. 4-heterocyclyl-1-acyl-piperidine derivatives of formula (I), their tautomers, diastereomers, enantiomers, hydrates and/or (hydrated) salts are new A and B each : N or CH; D : hydrogen or Me; E : hydrogen, fluoro, chloro, bromo, Me, Et or trifluoromethyl; X : CH2 or NH; R1>2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl or 5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl; R2>4-Ra-piperidin-1-yl, 4-Rb-piperazin-1-yl or 4-Rc-perhydro-1,4-diazepin-1-yl; Ra : piperidin-1-yl, piperidin-4-yl (optionally N-substituted by Me, methoxycarbonylmethyl or methylsulfonyl), dimethylamino, piperazin-1-yl (optionally 4-methyl substituted), pyrrolidin-1-yl, perhydro-1,4-diazepin-1-yl (optionally 4-methyl substituted) or 4-fluorophenyl; Rb : piperidin-4-yl (optionally 4-methyl substituted), pyridin-4-yl or 4-fluorophenyl; Rc : piperidin-4-yl, optionally N-methyl substituted) . An independent claim is also included for 5 methods of preparing (I). [Image] - ACTIVITY : Antimigraine; Analgesic; Antidiabetic; Cardiant; Antidiarrhea; Dermatological; Antiinflammatory; Antiarthritic; Antiallergic; Antiasthmatic; Antibacterial; Immunosuppressive; Gynecological; Cytostatic. No details of tests for these activities are given. - MECHANISM OF ACTION : (I) are selective antagonists of calcitonin-gene related peptide, with IC50 below 104> nM.
WO2012053787A3 Aryloxy phenoxy acrylic compound having hif-1 inhibition activity, method for preparing same, and pharmaceutical composition containing same as an active ingredient The present invention relates to a compound having HIF-1 inhibition activity, to a method for preparing same, and to a pharmaceutical composition containing same as an active ingredient. The compound of the present invention exhibits anticancer activity by inhibiting the activity of HIF-1, which is a transcription factor that plays a significant role in cancer cell growth and metastasis, and does not indicate non-selective, cytotoxic anti-tumour activity. Accordingly, the compound or a pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumours such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.
US20050255124 HCV E1E2 vaccine compositions HCV E1E2 compositions comprising E1E2 antigens, submicron oil-in-water emulsions and/or immunostimulatory nucleic acid sequences are described. The compositions can be used in methods of stimulating an immune response in a vertebrate subject.
CN101015501A Injection composition of fat milk, amino acid and glucose packed with three-cavity bag and preparing method thereof The invention discloses an injection composition packaged in a three-cavity bag. The three cavities separated by diaphragm are respectively filled with fattiness milk injection, compound amino acid injection, and glucose injection. The using method is crimping each cavity in turns, or divulging the isolating bar in each cavity to mix the injections for venoclysis so as to avoid the venture of microorganism and particulates pollution in traditional mix processing. The mix processing can be carried out under any environmental condition which qualifies the small hospital without aseptic preparation condition to use the nutrition, highly reduce the untoward reaction such as transfusion heater response, sanguis infection, and blood poisoning due to traditional mix processing.
WO2008116024A3 Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics Combinations of 5-HT2A inverse agonists or antagonists such as pimavanserin with antipsychotics such as risperidone are shown to induce a rapid onset of antipsychotic action and increase the number of responders when compared to therapy with the antipsychotic alone. These effects can be achieved at a low dose of the antipsychotic, thereby reducing the incidence of side effects. The combinations are also effective at decreases the incidence of weight gain and increased glucose or prolactin levels caused by the antipsychotic.
US20050004130 New metabotropic glutamate receptor compounds The present invention relates to new compounds of formula I, wherein P, Q, X1, X2, R1, R2, R3, R4, m and n, are as defined as in formula I, or N1-oxides, salts, solvates or solvated salts thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
US7122537 Which has superoxide acitivity, catalase activity, and/or peroxidase activity; for treating cell or tissue damage; improved organ, cell or tissue culture; diseases such as neurodegenerative diseases This invention provides antioxidant cyclic salen-metal compounds, compositions of such antioxidant cyclic salen-metal compounds having superoxide activity, catalase activity and/or peroxidase activity and methods of using such antioxidant cyclic salen-metal compositions to treat or prevent a disease associated with cell or tissue damage produced by free radicals, such as superoxide.
US7241791 Substituted 4-(indazol-3-yl)phenols This invention provides compound of formulae I or II having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined in the specification or a pharmaceutically acceptable salt thereof which are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatiod arthritis.
CN101269074A Pharmaceutical composition containing right-handed rebeprazole and preparation method thereof The invention relates to a drug compound containing D-rabeprazole and the preparation method thereof. The drug compound is prepared by adopting D-rabeprazole as the main active ingredient and mixing with auxiliary ingredients acceptable in pharmacy. The drug compound can be made into any solid formulations, such as tablets, capsules, granules, dispersible tablets, chewable tablets, buccal tablets, effervescent tablets, effervescent granules and so on, wherein, the unit preparation content of D-rabeprazole is 2 to 40mg and 10 to 20mg is preferable. The drug compound of the invention containing D-rabeprazole can be used for treating various types of digestive tract diseases, in particular peptic ulcers.
CN1583063B Extraction of effective components from frankinscene and its preparation and use The invention provides a method for extracting active component from olibanum, an extract preparation and use. The method comprises the following steps: taking the olibanum(including mix-fried olibanum) as raw material, firstly crushing the raw material into 40-60mesh, putting in an extract device, adding 60-95% of ethanol with the weight of 1-10time of the raw material crude powder, concentrating the leach liquor into an extract; adding 1-10% of sodium bicarbonate solution or 1-5% of sodium hydroxide into the extract, stirring and extracting for 1-5 times under a normal temperature and a normal pressure, each time for 0.5-3h, then allowing to stand for 1-10h, collecting precipitation layer and dissolving with ether; then respectively gradiently extracting by using 1-5% of sodium hydroxide and 1-10% of solidum bicarbonate solution, and adjusting pH of the alkaline water layer to 2-6 by using acid, then extracting for 1-3 times by using ether, reclaiming the ether, and obtaining active component extract crude product of the olibanum. The inventive extracted olibanum extract is used for anti-inflammatory and curing rheumatism impediment pain.
CN101486743B Novel iridoid compound with anti-Alzheimer's disease function The invention provides a novel iridoids compound with anti-senile dementia function and discloses a serial of iridoids compounds with the structural formula (I), the application of the compounds in preparing medicaments applied to the prevention or treatment of nervous system degenerative disorders such as senile dementia and the like, the medical compositions containing the compounds and a preparation method of the compounds. The structural formula (1) is as shown above, wherein each group is defined in the description.
WO2009087305A1 6-aryl/heteroalkyloxy benzothiazole and benzimidazole derivatives, method for preparing same, application thereof as drugs, pharmaceutical compositions and novel use in particular as c-met inhibitors The invention relates to novel products of the formula (I) in which : R is H, HaI or AIk; A is NH or S; R5 is H or Alk optionally substituted by one or more HaI; R6 is an optionally substituted aryl or heteroaryl; W is H or COR7 in which R7 is a cycloalkyl, an optionally substituted alkyl, an optionally substituted alkoxy or NR1 R2 with one of R1 and R2 being H or alk while the other of R1 and R2 is a cycloakyl or an optionally substituted alkyl; or R1 and R2 form together with N to which they are bonded; a cyclic radical optionally including one or more optionally substituted O, S, N and NH; the invention also relates to said products in any of their isomer forms or as salts, and they can be used as drugs, in particular as c-Met inhibitors.
WO2013024002A1 PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
EP2592073A2 Human protein tyrosine phosphatase inhibitors and their use The present application relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present application further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.
CN103655563A Method of inhibiting mutant C-KIT The present invention includes a method of reducing or inhibiting the kinase activity of C-KIT mutant tyrosine kinase activity in a cell or a subject, and the use of such compound for treating mutant C-KIT driven cell proliferative disorder(s) in a subject related to using a compound of the present invention: or pharmaceutically acceptable salt thereof.
US20100166857 Pharmaceutical dosage forms and methods of manufacturing same The invention provides solid dispersions of at least one insoluble active pharmaceutical ingredient, pharmaceutical dosage forms comprising the solid dispersions, and methods of manufacturing same. In an embodiment, a solid dispersion of the present invention includes a plurality of coated particles comprising inert particles with a coating, wherein the coating comprises an insoluble active pharmaceutical ingredient dispersed in a hydrophilic polymer, and wherein the inert particles comprise nonpareils; and a plurality of granules comprising an insoluble active pharmaceutical ingredient with at least one pharmaceutically acceptable excipient. In an embodiment, the insoluble active pharmaceutical ingredient in the coating and the insoluble active pharmaceutical ingredient of the granules are the same type. A solid dispersion of the present invention may optionally be encapsulated in capsules or compressed into a tablet. Also disclosed are methods of making solid dispersions and methods of reducing plasma triglyceride and increasing high-density lipoprotein employing the solid dispersion.
CN101899116A Non-invasive high-penetrability epidermal growth factor and application thereof The invention relates to a non-invasive high-penetrability epidermal growth factor (EGF) and application thereof, in particular to protein obtained by fusing protein transduction peptides with active fragments of human EGF and a nucleic acid molecule containing the nucleotide sequence coding the fragment. The invention relates to an expression vector containing the nucleic acid molecule. The EGF can treat virus infection, specifically kill tumor cells and treat neurodegenerative diseases, etc.
CN1989993A Effective alopecia-preventing liniment The invention discloses an externally-used medicinal liniment for treating alopecia, which is prepared from compositions of meta-dihydroxybenzene, mentha camphor, 2-hydroxybenzoic acid, ammonium carbonate, castor oil, distilled water and 50% ethanol through specific processes. The medicament is mainly used for treating hair loss, hair fracture and alopecia areata.
CN103505442A Target nano lipid core micelle used for carrying docetaxel, and preparation method and applications thereof The invention discloses a target nano lipid core micelle used for carrying docetaxel, and a preparation method and applications thereof. The target nano lipid core micelle is obtained by RGD peptide surface modification of a nano lipid core micelle used for carrying docetaxel; the nano lipid core micelle used for carrying docetaxel is prepared via thin-film hydration method of a polyethylene glycol polymer with methoxyl end groups, a polyethylene glycol polymer with maleimide end groups and docetaxel. It is confirmed by experiment results that: the target nano lipid core micelle is of a uniform spherical shape, is composed of discontinuous nanoparticles, is small in particle size and uniform in distribution, is capable of changing pharmacokinetics characteristics of docetaxel, and possesses obvious sustained release effect, excellent compatibility with blood plasma, and no obvious toxicity on cells. In addition, the preparation method is simple, is suitable for scale production, and possesses relatively promising clinical application prospect and high social benefits.
US20080138288 Combinations for treatment of neovasculature Long-term treatment of conditions associated with neovasculature is effected by combining targeted acute antiangiogenic agent treatment with chronic treatment with an additional drug.
CN103007210A Preparation method of poria cocos, bamboo leaves and honey paste The invention relates to a preparation method of poria cocos, bamboo leaves and honey paste. The method comprises putting the poria cocos, pinellia ternate, ephedra stem and cassia twig into a pan, adding water, immersing, decocting, filtering, condensing, adding the honey, and decocting until boiling to obtain the paste. The product can moisten lung, reduce phlegm, and remove lung heat, and has very significant treatment effect for patients undergone an unhealed cough for a long time.
CN1840538A 1-(2'-deoxy-2'-fluoro-3'-O-amino acid ester-beta-L-furyl arabinosyl)-5-methyl uracil and its application The related 1-(2'-deoxy-2'-fluo-3'-O-amino cid ester-beta-L-arabinofuranose)-5-methylouracil with structure as formula I and its medicinal salt is preparated by the 1-(2'-deoxy-2'-fluo-3'-O- amino cid ester-beta-L-arabinofuranose) basic radical. The compound with formula I and its salt or the second antiviral drug can be used to cure and/or prevent acute and chronic HBV or EBV or disease led by HCV.
US20120177716 Methods for Making Controlled Delivery Devices Having Zero Order Kinetics A method of making an injectable or implantable active agent delivery device capable of delivering a diagnostic, therapeutic, and/or prophylactic agent to a desired targeted site having orifice(s) on the surface is disclosed herein providing unidirectional release of the agent at a controlled desirable rate. The agent may include, but is not limited to, drugs, proteins, peptides, biomarkers, bioanalytes, and/or genetic material. The technology of the invention is based on parallel processing to fabricate micro-holes on tubes employing photo-lithography and reactive ion etching techniques and also incorporates a simple molding method to form the micro-holes on flexible polymer tubes, including bio-degradable tubes. The parallel processing method of the instant invention is fast, economical and well suited for mass production. The developed device, due to its composite structure, has the ability to combine several release mechanisms, leading to zero-order release kinetics for most of the time.
WO2006051407A1 Azabenzoxazoles for the treatment of cns disorders The present invention relates to α7 nicotinic receptor agonists of formula I as described herein and to a method for treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal an α7 nicotinic receptor agonist of formula I as shown herein. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant α7 nicotinic receptor agonist of formula I.
CN101531682A Metal coordination complex and method for preparing same The invention discloses a metal coordination complex, and relates to the field of chemistry. The metal coordination complex is for preparing a complex with potential medicinal value, and is characterized in that potassium tetrachloropalladate or potassium tetrachloroplatinate and 2,2'- bipyridyl-5,5'-dicarboxylic acid have reaction according to molar ratio under the hydrothermal condition to obtain a target complex. A preparation method comprises the following steps: a mixture of the potassium tetrachloropalladate (the potassium tetrachloroplatinate), the 2,2'- bipyridyl-5,5'-dicarboxylic acid and water is stirred for 40 minutes at the room temperature; and subsequently, the mixture is transferred to a polytetrafluoroethylene liner of a hydrothermal reaction kettle (the size of the liner is between 25 and 50 ml), is kept at constant temperature of between 100 and 120 DEG C, and is cooled to the room temperature to prepare a [PdLCl2].2H2O yellow rhombic {[PtLCl2].2H2O brown rectangular} crystal. The prepared complex has clear composition and a clear molecular structure and has potential medicinal application value.
US20100105631 Inositol Compounds and Uses of Same in the Treatment of Diseases Characterized by Abnormal Protein Folding or Aggregation or Amyloid Formation, Desposition, Accumulation or Persistence Inositol derivatives are described that are represented by the structural formula I wherein X is a radical of scyllo-inositol wherein one or more of R1, R2, R3, R4, R5, and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl, or carboxamide and the other of R1, R2, R3, R4, R5, or R6 are hydroxyl, or pharmaceutically acceptable salts thereof. The compounds, compositions comprising same and methods using same are described for use in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, desposition, accumulation or persistence.
EP2493482A1 Therapeutic gas for the treatment of mitochondrial disorders The use of gaseous oxygen for the production of a therapeutic gas for inhalation by a patient who has been identified as a person with a mitochondrial disorder or a coenzyme Q10 deficiency, for the treatment of mitochondrial disorders or Q10 deficiencies is disclosed. For the first time a non-invasive method is disclosed, upon what the body's own level of Q10 can be raised significantly without further interventions.
WO2012039469A1 Method for screening binding inhibitor of rage and age Provided is a method for screening a binding inhibitor of RAGE and AGE focused on the new activity of β-amyloid peptide. Provided is a method for screening a binding inhibitor of RAGE and AGE by sorting candidate compounds inhibiting the activity affecting the binding affinity of RAGE and AGE of β-amyloid peptide through finding, for the first time, that the β-amyloid peptide makes the binding of RAGE and AGE change to high binding affinity. The binding inhibitor obtained by this screening method can be used as a therapeutic agent for any diseases or symptoms caused by the binding of RAGE and AGE in which β-amyloid peptide involves. Especially, the binding inhibitor is capable of contributing to the development of the therapeutic drug for Alzheimer's disease focused on the new mechanism.
CN1562056A Slow and control release preparation for thromus A slowly-releasing (or release-controllable) Xusaitong for treating thrombus contains sanchisaponin and slow-releasing additive.
US20130195882 Mcpip protection against osteoclast production Disclosed herein are methods of treating a patient at risk of developing an inflammatory joint disease. In exemplary embodiments, the method involves inhibiting MCPIP levels in a patient in need, wherein said patient in need is exhibiting pre-arthritic or pre-osteoporotic symptoms.
US20100048670 Stable and Long-Lasting siRNA Expression Vectors and the Applications Thereof The invention relates to a siRNA expression vector that can inhibit or eliminate the expression of a target gene in a mammalian cell, said vector comprising: a bacterial cassette containing a bacterial origin of replication and a bacterial selection marker M1; a eucaryotic cell selection cassette comprising a marker M2 for selecting eucaryotic cells under the control of an appropriate promoter; a cassette EBV comprising at least one fragment of the antigen EBNA-1, at least one fragment FR, and at least one fragment of the region DYAD; and a siRNA transcription cassette comprising at least one region coding for a siRNA corresponding to the target gene to be inhibited or eliminated, under the control of elements for regulating transcription in mammalian cells, said regulating elements including at least one promoter capable of transcribing a siRNA in mammalian cells, and a transcription terminator. The invention also relates to the applications of one such expression vector.
CN103083265A Nitrendipine tablet and preparation method thereof The invention relates to a nitrendipine tablet and a preparation method thereof. The nitrendipine tablet comprises, by weight, 1 part of nitrendipine, 1.0 to 5.0 parts of polyvinylpyrrolidone, 0.05 to 0.25 parts of polyethylene glycol, 0.05 to 0.4 parts of hydroxypropyl methyl cellulose, and 0.5 to 2.0 parts of polysaccharide. The preparation method comprises the following steps of dissolving nitrendipine in a solvent, adding a part of auxiliary materials into the solution, fully mixing to obtain a homogeneous system, wherein nitrendipine is distributed in a molecular state or an amorphous state, and adding the rest of the auxiliary materials into the mixture to obtain the nitrendipine tablet. The nitrendipine tablet has high bioavailability and can be fully and easily absorbed by organisms after oral administration.
WO2006130666A3 Medicaments and methods combining a hcv protease inhibitor and an akr competitor Disclosed are medicaments, pharmaceutical compositions, pharmaceutical kits, and methods based on combinations of a hepatitis C virus (HCV) protease inhibitor and an aldo-keto reductase (AKR) competitor, for concurrent or consecutive administration in treating, preventing, or ameliorating one or more symptoms of HCV, treating disorders associated with HCV, or inhibiting cathepsin activity in a subject.
CN102824302A Topiramate sustained release preparation and preparation method thereof The invention relates to a medicine sustained release preparation, and particularly relates to a topiramate sustained release preparation and a preparation method thereof. The topiramate sustained release preparation is prepared by sustained release particles and pharmaceutical auxiliary materials, wherein the sustained release particles comprise 15-30% of topiramate, 30-60% of an ion-exchange resin, 12-25% of an impregnant and 5-15% of a sustained release coating material. The topiramate sustained release preparation has stable and effective plasma concentration which is lower than the peak concentration of a quick release preparation, reduces incidence rate of side reactions, and can control epileptic seizures well. The topiramate sustained release preparation is taken once every day, and employs the ion ion-exchange resin, so that unpleasant taste of topiramate can be covered; and adaptability for patients is increased. The topiramate sustained release preparation can be well-received by doctors and patients.
CN102106881A Medicament for treating shingles and preparation method thereof The invention discloses a medicament for treating shingles and the preparation method thereof. The medicament for treating the shingles is prepared from the following raw materials in parts by weight: 10 to 20 parts of natural indigo, 5 to 13 parts of rabiagar and 5 to 15 parts of dried alum. The preparation method comprises the following steps: weighting the indigo naturalis, the realgar and the dried alum according to the mixture ratio of the raw materials; respectively grinding the three raw materials into powder; uniformly mixing the ground powder to obtain the mixed powder; then adding tea water into the mixed powder; and uniformly mixing to obtain the medicament for treating the shingles. Proved by clinical application, that is, after the medicament for treating the shingles disclosed by the invention is used by patients for about half a month, all symptoms of the shingles can be relieved; after the medicament is used, the shingles can be basically cured and is not easy to recur; and the medicament has the advantages of remarkable effect, no toxic or side effect, effective rate of 98 percent, cure rate of 90 percent, short treatment course and low expense.
US20090093502 Improved lactate (leucine, arginine, methyl pyruvate, and methyl succinate) usage is accomplished through lactate precursors, adrenergic receptor agonists and insulinotropic agents The present invention relates to a method of improving the energy status of an individual by enhancing the usage of lactate. Improved lactate usage is accomplished through a composition comprising lactate precursors, adrenergic receptor agonists and insulinotropic agents.
WO2014065510A1 Novel rotenone derivatives and a use thereof The present invention relates to a novel rotenone derivative and a use of the same. Particularly, the present inventors identified the novel rotenoisin A and B which were the compounds with no toxicity and prepared by irradiation with gamma ray onto rotenone represented by the following formula 1 and further confirmed that the novel rotenone derivative significantly inhibited pancreatic lipase activity and preadipocyte differentiation. The novel rotenone derivative of the present invention can be effectively used as a composition for the prevention and treatment of obesity and as a composition for health functional food for the prevention and improvement of obesity: [Formula 1] (In formula 1, R1 and R2 are as defined in this description).
US7553482 Preventing atherosclerotic disease, bone disorders by administering iron(III) oxide hydroxide-carbohydrate complexes; for reducing the calcium phosphate product, calcium level in the blood; side effect reduction; controlling blood metal concentration The invention relates to the use of an adsorption material which has been modified with polynuclear metal oxide hydroxides for influencing the calcium level and, in particular, for treating or/and preventing atherosclerotic vascular diseases or/and disturbances of bone metabolism.
EP1721604A1 Stable capsule preparation A capsule in which an unstable active ingredient has been stabilized is obtained by lowering the moisture content of a solid preparation (granules, subtilis, tablets, etc.) containing a chemical unstable to moisture such as an imidazole PPI compound by drying or the like, and then filling in a capsule comprising a water-soluble polysaccharide such as pullulan as the main component or a PEG-containing gelatin capsule. For the further stabilization, the capsule per se may be dried. The capsule preparation thus obtained is a stable capsule preparation with the use of a capsule being stable at a low moisture content which contains a chemical unstable to moisture such as an imidazole compound.
US20110207798 Method for treating breast cancer using adenine nucleotide translocator 2 (ant2) sirna or ant2 shrna The present invention relates to adenine nucleotide translocator 2 (ANT2) siRNA (small interfering RNA) or ANT2 shRNA (short hairpin RNA) suppressing the expression of ANT2 gene expression and anticancer agent containing the same. Furthermore, the present invention relates to methods for treating breast cancers or stem cells of a breast cancer by treating the same with ANT2 siRNA or ANT2 shRNA. In addition, the invention provides a method for inhibiting metastasis of breast cancer cells with ANT2 siRNA or ANT2 shRNA.
CN102634478A Action of improving function of endothelial progenitor cells by tripterine The invention relates to an action of improving a function of endothelial progenitor cells (EPC) by tripterine, and particularly relates to a method for culturing the endothelial progenitor cells in vitro. The method comprises the following step of culturing the endothelial progenitor cells under the coexistence of the tripterine or medically accepted salt or ester of the tripterine, or a derivant of the tripterine. According to the method, the shortcoming of the function of the EPC is overcome, and the migration capacity of the EPC and the capacity of forming a blood vessel network are improved.
US20130280348 Carbon dioxide and saline nasal delivery methods and treatments Methods for treating ailments in a patient in need thereof includes the step of directing a therapeutic, non-inhaled dosage to at least one nasal cavity of the patient through a flow regulating device while the patient refrains from inhaling. The dosage includes a saline fluid and a gas containing carbon dioxide, wherein the therapeutic, non-inhaled dosage is delivered at a flow rate from 1 cc/sec to 20 cc/sec for a duration of 2 to 30 seconds.
EP2687516A1 Inhibitors of C-FMS Kinase The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
WO2007071653A1 Use of aminoalcohol derivatives for the treatment of overactive bladder The present invention relates to the use of new beta-agonists of general formula (Ia) or (Ib) wherein the groups R1 to R12 and R1 to R7, respectively, have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, for preparing a medicament for the treatment of overactive bladder.
CN103285078A Comfortable cream The invention discloses a comfortable cream which comprises water, glycerol, stearic acid, glyceryl stearate, cetostearyl alcohol, polysorbitol-80, chrysanthemum indicum extract, menthol, cassia tora seed extract, red-rooted salvia root extract, common groundsel extract, pearl powder, thymol crystals, borneol, borax, triethanolamine, sodium hyaluronate and ethylparaben. The comfortable cream is simple in preparation and remarkable in effect, can be used for massaging eyes and relieving eye fatigue, and has a function of relieving the visual fatigue caused by overuse.
WO2009060292A2 Smac mimetic compounds as apoptosis inducers The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
CN101940553A Folic acid-vincristine targeted and slow-released nano-microspheres, prepared method and application thereof The invention discloses folic acid-vincristine targeted and slow-released nano-microspheres, a prepared method and an application thereof. The preparation method comprises the steps of: dissolving the polylactic acid-glycollic acid in the dichloromethane and acetone to form the oil phase; dissolving the polyethylene glycol and the hydroxyethylcellulose in the water solution of vincristine and stirring to form the inner water phase, and adding the inner water phase into the oil phase dropwise to form the water/oil initial emulsion solution; adding the water solution of O-carboxymethyl chitosan octadecyl hyamine containing the hydroxyethylcellulose and the connected folic acid into the initial emulsion solution to form the water/oil/water composite system; stirring and volatilizing the organic solvent to obtain the solidified microspheres; centrifuging the solidified microspheres, removing the separated large-sized microspheres, centrifuging again to obtain the separated solid microspheres, washing and dirying to obtain the discloses folic acid-vincristine targeted and slow-released nano-microspheres. The discloses folic acid-vincristine targeted and slow-released nano-microspheres of the invention have good effect, high local drug concentration, long action time and less adverse reaction.
WO2008010566A1 Crystalline polymorphism of 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid Disclosed is a novel crystal of 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid anhydride or monohydrate. Specifically disclosed is a type-I or -II crystal of 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid anhydride, which has a specific diffraction peak in a powder X-ray diffraction spectrum. Also specifically disclosed is a type-II or -III crystal of 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid monohydrate, which has a specific diffraction peak in a powder X-ray diffraction spectrum.
US20110207779 Process for the preparation of esomeprazole magnesium The present invention relates to a process for the preparation of esomeprazole magnesium containing R-isomer greater than about 0.1% by wt. In particular, the present invention relates to a process for the preparation of esomeprazole magnesium dihydrate containing R-isomer greater than about 0.1% by wt.
US6897310 1,5-methylene-3-benzazepines used in treatment of neurological and psychological disorders,especially withdrawl from nicotine addiction Pharmaceutical compositions comprising compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, in combination with another therapeutic agent and methods of using such combinations in the treatment of neurological and psychological disorders.
WO2012038492A1 Novel substituted amino-, imino-1,2,4 triazine derivatives The invention relates to novel compounds of amino-, imino-1,2,4 triazine derivatives of formula (I) and to the use of the same as medicament.
CN103102377A Novel crystal form of erythromycin A-ring 11,12-carbonic ester, pharmaceutical composition containing novel crystal form B, and application thereof The invention relates to a novel crystal form of erythromycin A-ring 11,12-carbonic ester, a pharmaceutical composition containing the novel crystal form B, and an application of the pharmaceutical composition, and in particular, relates to a novel crystal forms of which the name and structure is B, C or D, of the erythromycin A-ring 11,12-carbonic ester. The novel crystal form has an X-ray powder diffraction pattern shown in a table 1, a table 2 or a table 3 and a diagram 1, a diagram 3 or a diagram 5, and an IR (Infrared Ray) radiation absorption spectrum shown in a diagram 2, a diagram 4 or a diagram 6. The invention further relates to the pharmaceutical composition containing the novel crystal form B of the erythromycin A-ring 11,12-carbonic ester, and as well as the medical application of the pharmaceutical composition.
EP2536727A1 Deuterated pyrrolopyrimidine compounds as inhibitors of cdk4/6 The invention is directed to novel deuterated pyrrolopyrimidine compounds of formula (I) wherein R1 and R2 are defined below and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
CA2559465A1 Herbal therapy for the treatment of asthma The present invention provides herbal formulas, and compositions thereof, that can treat or reduce the severity, intensity, or duration of asthma and asthma-related symptoms. The compositions may optionally include one or more adjuvants, cytokines, encapsulating materials, or pharmaceutically acceptable carriers or excipients, and may be administered prior to, during, or after the development of asthmatic symptoms in a patient in need thereof.
US20050203103 Arylalkyl indoles having serotonin receptor affinity useful as therapeutic agents, process for their preparation and pharmaceutical compositions containing them The present invention relates to novel tetracyclic arylalkyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel tetracyclic arylalkyl of the general formula (I), their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention also relates to process/es for preparing such compound/s of general formula (I), composition/s containing effective amount/s of such a compound and the use of such a compound/composition in therapy.
CN103193780A Use of 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives in preparation of drug for prevention or treatment on cerebral hemorrhage The invention discloses a use of 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives in preparation of a drug for prevention or treatment on cerebral hemorrhage. Through a self-created computer-assisted drug molecule design program and virtual screening, it is shown that the 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives have a ROCK1 protein inhibitory activity and can be used for treating cerebral hemorrhage. Through further biological activity detection of the screened 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound, it is shown that the screened 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound has an obvious ROCK1 protein inhibitory activity and has good prevention and treatment effects in an atorvastatin-induced zebra fish cerebral hemorrhage model.
WO2004064764A3 Substituted alkyl amido piperidines This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.
WO2011017519A2 Inhibitors of methionine aminopeptidases and methods of treating disorders The invention is directed towards novel naphthoquinone and naphthothiazole compounds, and methods of treating disorders related to MetAP, including tuberculosis and bacterial infection, using various naphthoquinone, hydroxyquinonline, and naphthothiazole compounds.
CA2609391A1 Quinazolinones Disclosed are compounds of formula (I), wherein R, R1, R2, R3, R4, R5, R6, R7, R8, Z1, Z2, Z3, k, and Y1 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.
US20130004590 Zinc oxide/acid containing compositions and methods for treating and/or preventing enzymatic irritation Compositions and methods for treating and/or preventing conditions such as diaper rash and atopic dermatitis are disclosed. The compositions and methods are particularly useful in the treatment and prevention of diaper rash and diaper dermatitis caused by the prolonged contact of human skin with body waste. The methods employ the topical application of a trypsin-inhibiting agent to the area in need of such treatment, or the area where prevention is desired. The trypsin-inhibiting agent is preferably zinc oxide in combination with an acid so as to release a specified divalent cation, i.e., zinc.
CN102827151A 7-methoxy-2, 8-bis (3-methylbut-2-enyl) xanthone-1, 3, 6-triyl tripyrazine-2-carboxylate, and semi-synthesis method and medicinal application thereof The invention relates to a novel compound which is synthesized by using 1, 3, 6-Trihydroxy-7-methoxy-2, 8-bis (3-methyl-2-butenyl)-9H-xanthen-9-one and 2-pyrazinecarboxylic acid as raw materials under the existence of catalyst through esterification. The chemical name of the novel compound is 7-methoxy-2, 8-bis (3-methylbut-2-enyl) xanthone-1, 3, 6-triyl tripyrazine-2-carboxylate. The yield reaches more than 80 percent. The 7-methoxy-2, 8-bis (3-methylbut-2-enyl) xanthone-1, 3, 6-triyl tripyrazine-2-carboxylate has a wide application scope in preparation of anti-tumor drugs.
CN101513423A Application of oleanane-28-acid-2,9(11),12-triene in preparing medicament for treating skin diseases The invention discloses application of oleanane-28-acid-2,9(11),12-triene in preparing a medicament for treating skin diseases, and provides a pharmaceutical composition. The pharmaceutical composition is characterized by comprising the oleanane-28-acid-2,9(11),12-triene (I) which is taken as an active component and one or more medicinal accessories. In the pharmaceutical composition provided by the invention, the medicinal accessories are all administrative accessories which are suitable for the skin or mucosa.
WO2009063476A1 A crystalline form of atorvastatin hemi magnesium salt and a process thereof The present invention provides crystalline forms B4 and B5 of atorvastatin hemi magnesium salt. In addition, it also provides a process for preparation of crystalline forms B4 and B5 of atorvastatin hemi magnesium salt.
US20100041631 Methods and agents for treating tuberculosis The present invention relates to the treatment of tuberculosis (mycobacterial infections) by the use of KshAB complex inhibitors, or a KstD molecule, or a HsaAB complex, or a HsaC molecule, or a HsaD molecule. The application also includes a method for identifying an inhibitor or modulator of the previously mentioned molecules and complexes.
WO2014106050A1 Compositions comprising lithium This invention relates to compositions comprising lithium and methods of their use.
CN102985421A Naphthridine derivatives as pi3k inhibitors for the treatment of cancer and immune - inflammatory diseases Described are compounds of formulae (I) and (II) or a pharmaceutically acceptable salt thereof, wherein R1 is a nitrogen-containing 5 to 7-membered heteroaryl or heterocycle; and R2 and R3 are each independently (LQ)mY. The compounds are PI3K inhibitors and are useful for the treatment of cancer and immune-inflammatory diseases.
WO2012129491A1 Trpv3 modulators Disclosed herein are modulators of TRPV3 of formula (I) wherein X1, X2, R1, R2, Rx, and n are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
CA2741537A1 Quinoxaline-based lxr modulators Disclosed are quinoxaline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): wherein: each of L1 and L2 is, independently, a bond, -O- or -NH-; R2 is C6-C10 aryl or heteroaryl including 5-10 ring atoms, each of which is (i) substituted with 1 R9, and (ii) optionally further substituted with from 1-4 Re; and each of R4 and R5 is, independently (i) hydrogen; or (ii) halo; or (iii) C1-C6 alkyl or C1-C6 haloalkyl, each of which is optionally substituted with from 1-3 Ra; and R1, R3, R6, R9, Ra and Re are defined herein. In general, these compounds can be used for treating or preventing one or more diseases, disorders, conditions or symptoms mediated by LXRs.
CA2745959A1 Dihydropyrimidopyrimidine derivatives The invention relates to compounds represented by the general formula (I) and the like. In the formula, Ar1 denotes an aryl or heteroaryl group which may have a substituent; R1 denotes a hydrogen atom, or denotes a C1-C6 alkyl, aryl, aralkyl or heteroaryl group which may have a substituent; R2 denotes an aralkyl group or a group represented by the formula (a); and R3 denotes a hydrogen atom or a C1-C6 alkyl group. The compounds of the invention have an excellent Weel kinase inhibitory effect, and therefore are useful in the field of medicine, especially in the field of treatment of various cancers.
WO2014149789A1 Combination of canagliflozin and probenecid for the treament of hyperuricemia The present invention is directed to methods for treating hyperuricemia and related disorders, comprising co-therapy with canagliflozin and probenecid.
WO2006123355A3 Novel statin derivatives The present invention provides novel statin derivatives and a facile process for preparation thereof selected from a group consisting of a compound of formula (I), wherein R is selected from a group consisting of -OH, -OR1, OCOR1, -OCHO, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, alkylaryl, heteroaryl, aralkyl, heterocycle having ring size between 3 to 6, -CN, -COOH, -COOR1, -CONHR1, -CONR1R2, -NH2, -NHR1, -NR1R2 halogen, -SH and -SR1; wherein R1 and R2 are independently selected from C1-C6 alkyl, alkylaryl, heteroaryl, aralkyl, heterocycle having ring size between 3 to 6, C2-C6 alkenyl and C2-C6 alkynyl, or R1 and R2 together with the carbon atom to which they are attached from a heterocycle with a ring size from 3 to 6, ------ represents either α or β-susbstituent, and pharmaceutically acceptable salt thereof. The compounds have anti-hyperlipidimic anti-hypercholesterolemic and antiinflammatory activity.
US20110269779 Methods and compositions for treatment of ophthalmic conditions The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating signal transduction by certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PB kinase in an ocular tissue. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.
CN102552143A Medicine composition containing pravastatin sodium fenofibrate liposome and preparation method of medicine composition The invention relates to a medicine composition containing a pravastatin sodium fenofibrate liposome and a preparation method of the medicine composition. The medicine composition comprises a pravastatin sodium fenofibrate liposome and at least one pharmaceutically acceptable vector, wherein the pravastatin sodium fenofibrate liposome comprises pravastatin sodium, fenofibrate, phospholipid and cholesterol. The medicine composition prepared by the pravastatin sodium fenofibrate liposome not only satisfies the requirements of Chinese Pharmacopoeia and has the advantages of faster dissolution, faster medicine efficacy, high bioavailability, good stability as well as worth of being widely promoted and applied when being compared with the common pravastatin sodium fenofibrate medicine composition.
US7279580 For prophylaxis and therapy of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders A class of 8-fluoro-3-phenylimidazo[1,2-α]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a —NH— or —OCH2— linkage, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
WO2011005886A1 Method of reducing multi-drug resistance using inositol tripyrophosphate Inositol trisphosphate (ITPP) causes normalization of tumor vasculature and is a particularly effective cancer therapy when a second chemotherapeutic agent is administered following partial vascularization. ITPP also treats, alone or in combination, multi-drug resistant cancers. ITPP can also be used to reduce the amount of a second chemotherapeutic drug required for anticancer activity. In addition, ITPP enhances immune response and treats hyperproliferative disorders.
US6949133 Portable oxygen concentrator A compact and highly portable combination pressure swing adsorption apparatus and product gas conservation device for medical use, to produce efficiently a gas with a high concentration of oxygen and to deliver the oxygen concentrated gas to a user at selectable times and in selectable doses.
CN102920701A Compound florfenicol preparation for treating swine respiratory tract infection diseases and preparation method thereof The invention discloses a compound florfenicol preparation for treating swine respiratory tract infection diseases and a preparation method thereof. The compound florfenicol preparation comprises florfenicol, flunixin meglumine, a composite organic solvent and an antioxidant agent, and the florfenicol and the flunixin meglumine are used as main drugs. The compound florfenicol preparation has anti-infection, anti-inflammation, antipyresis and analgesia effects, is dosed through subcutaneous injection and has remarkable effects for preventing and treating the swine respiratory tract diseases. The compound florfenicol preparation is exquisite in preparing process, controllable in quality, safe, reliable, convenient to use, low in cost, and suitable for being popularized and applied to cultivation industry.
CN102690240A Tolyltriazole alkene ether compounds and oxime ether compounds and preparation method and application thereof The invention discloses tolyltriazole alkene ether compounds and oxime ether compounds and a preparation method and application thereof, belongs to the field of medicinal chemistry, and particularly relates to new tolyltriazole antibacterial compounds which have the chemical structural general formulas in the specifications. The preparation method for the compounds is economic, simple, mild and effective. The obtained compounds have strong activity of inhibiting pathogenic bacteria escherichia coli; and the activity of the compounds is equivalent to that of a clinical medicine ofloxacin; and the compounds can be used for preparing new antibacterial medicines.
CN102908338A Preparation method of resveratrol microcapsule The invention discloses a preparation method of a resveratrol microcapsule, and the method comprises the following steps of: (1) dissolving resveratrol into a solvent, adding an emulsifying agent, and evenly mixing to obtain the core material solution by means of colloid mill; (2) adding water into chitosan, stirring, and swelling and dispersing the chitosan to prepare a wall material solution; and (3) stirring the core material solution and adding the core material solution into the wall material solution to obtain a mixed solution, homogenizing and emulsifying into white lactescence by means of colloid mill, adding a curing agent, continuously homogenizing by means of a colloid mill, and carrying out spray drying to obtain the resveratrol microcapsule with good dispersity. The resveratrol microcapsule prepared by the method provided by the invention is good in solubility and high in stability. The method provided by the invention is simple to operate, and easy for industrial production.
CN101045163A High molecular anticarcinogenic prodrug, its preparing method and use An anticancer high-molecular precursor medicine C-Spacer-P, where P is high- molecular pectin, C is an anticancer medicine containing amino radical or hydroxy radical, and Spacer is the spacing radical, is prepared by bonding the amino or hydroxy of an anticancer medicine with the hydroxy, carboxy, or hydroxymethyl of high- molecular pectin via spacing radical. It is an injection suitable for the solid cancer, and cancerous ascites or hydrothorax.
CA2780821A1 Mmp-13 inhibitors for the treatment of periodontitsis Described herein are compositions comprising a MMP-13 inhibitor, and methods of using the same.
US20110294881 METHODS FOR TREATING LOWER URINARY TRACT DISORDERS USING alpha2delta SUBUNIT CALCIUM CHANNEL MODULATORS WITH SMOOTH MUSCLE MODULATORS A method is provided for using α2δ subunit calcium channel modulators or other compounds that interact with the α2δ calcium channel subunit in combination with one or more compounds with smooth muscle modulatory effects to treat and/or alleviate the symptoms associated with painful and non-painful lower urinary tract disorders in normal and spinal cord injured patients. According to the present invention, α2δ subunit calcium channel modulators include GABA analogs (e.g. gabapentin and pregabalin), fused bicyclic or tricyclic amino acid analogs of gabapentin, and amino acid compounds. Compounds with smooth muscle modulatory effects include antimuscarinics, β3 adrenergic agonists, spasmolytics, neurokinin receptor antagonists, bradykinin receptor antagonists, and nitric oxide donors.
CN101249079B Andrographolide succinic acid half-ester natrium potassium salt and preparations The invention relates to a potassium sodium dehydroandroandrographolide succinate and a composition thereof. The composition contains andrographolide as pharmaceutically-active component, mannitol, calcium sodium EDTA, vitamin C and phosphate buffer. The composition for injection contains, per 1000, 20-200g of potassium sodium 14-dehydro-11,12- didehydroandrographolide-3,19-succinate, 3.868g of disodium hydrogen phosphate, 0.449g of sodium dihydrogen phosphate, 20-200g of mannitol, 0.5-5g of calcium sodium EDTA and 0.2-2g of vitamin C.
US20080167290 Particularly citalopram, escitalopram, fluoxetine, sertraline, paroxetine, fluvoxamine, venlafaxine, dapoxetine, nefazodone, imipramin, femoxetine or clomipramine; treatment of depression and other affective disorders The present invention relates to the use of a combination of Amoxapine and a serotonin reuptake inhibitor (SRI), or any other compound, which causes an elevation in the level of extracellular serotonin, for the treatment of depression and other affective disorders.
US20110212140 Pressure-sensitive adhesive composition applicable to nail and adhesive agent for nail The present invention aims at providing a pressure-sensitive adhesive composition applicable to nail, which shows superior adhesive performance (adhesive force, cohesion etc.), and superior drug releasability and drug stability, and an adhesive agent for nail, which uses this composition. The composition of the present invention contains a condensation polymer of a silicone resin and a silicone rubber. The composition of the present invention preferably contains not less than two kinds of condensation polymers having different resin/rubber ratios. The adhesive agent of the present invention has a support and an adhesive layer formed on one surface of the support, which contains the above-mentioned composition.
WO2007126362A1 Compounds that are agonists of muscarinic receptors and that may be effective in treating pain, alzheimer's disease and/or schizophrenia Compounds of Formulae I, or pharmaceutically acceptable salts thereof: [Chemical formula should be inserted here. Please see paper copy] I wherein X, R1, R2 and R3 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
US7101899 N-[4-[2-Ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide; adenosine A3 receptor antagonistic activity An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.
CA2363053C Clopidogrel bisulfate tablet formulation Pharmaceutical tablets comprising clopidogrel bisulfate and a lubricant selected from zinc stearate, stearic acid, and sodium stearyl fumarate.
US20120004219 Method of Inhibition of Respiratory Depression Using Positive Allosteric AMPA Receptor Modulators The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative.
WO2011143430A1 Indazole inhibitors of kinase The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,formula (I) wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.
US20090136474 Stabilized Protease Composition A composition is provided, which comprises a serine protease; a reversible inhibitor of said serine protease; and a stabilizing agent M having the formula I: Also provided are uses of the composition as a medicament, and other uses and methods employing its various properties.
WO2013179049A1 Spiro derivatives as voltage - gated sodium channel modulators The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
CN101607959A Dihydro quinolinone derivative, preparation method thereof and medicine composition taking same as main active ingredient The invention provides a novel dihydro quinolinone derivative, namely a compound shown as the formula (I) or the salt of the compound, which is pharmaceutically acceptable and described as the right formula; wherein n can be any number between 1 and 6, and A can be the formula (II) or the formula (III) with the structure shown as the right formula. The medicine composition containing the compound shown as the formula (I) has good curative effect on treating mental diseases caused by central nervous system dopamine and 5-hydroxytryptamine neurotransmitter disorder.
US20110274738 Functionalized chemically inert polymers for coatings Provided herein are methods for functionalizing a polymer for forming a coating and coatings and devices formed thereof or for functionalizing a coating or device surface including an polymer.
US7202255 Substituted [1,4] benzodioxino[2,3-e] isoindole derivatives, method for preparing and pharmaceutical compositions containing same Compounds of formula (I): wherein: A is as defined in the description, Y represents a group selected from an oxygen atom and a methylene group, R2 represents a hydrogen atom and in that case: R3 represents a group selected from a hydrogen atom and the groups linear or branched (C1–C6)alkyl, aryl, aryl-(C1–C6)alkyl (in which the alkyl moiety is linear or branched) and SO2CF3, or R2 and R3 form a bond, R1 represents a group selected from a hydrogen atom and the groups linear or branched (C1–C6)alkyl, aryl and aryl-(C1–C6)alkyl (in which the alkyl moiety is linear or branched) or a linear or branched (C1–C6)alkylene chain, Z1 and Z2 each represent a hydrogen atom or Z1 and Z2, together with the carbon atoms carrying them, form a phenyl group. Medicaments.
CN101697962A Process for preparing matrine-loaded magnetic chitosan microspheres The invention discloses a process for preparing matrine-loaded magnetic chitosan microspheres, which is characterized in that: a chemical precipitation method is used to prepare magnetofluid; an ion condensation method is used to preparing the matrine-loaded magnetic chitosan microspheres; the microsphere particle sizes are distributed normally and evenly; in the course of the process, static electricity triggers a physical crosslinking reaction to prevent toxic reagent from being introduced in a chemical crosslinking process so as to avoid unnecessary influences; and the obtained microspheres belong to a magnetic targeted medicament delivery system and have the characteristics of strong targeting, biodegradability, high efficiency and low toxicity.
US20130059854 Dosage Form for Insertion Into the Mouth Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, particularly anti-migraine agents to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.
CA2202775C Method for treating anxiety The present invention provides a method for treating anxiety in humans using heterocyclic compounds.
CN102614496A Wood frog bone high-calcium tablets and preparation method thereof The invention discloses wood frog bone high-calcium tablets and a preparation method thereof, and relates to calcium tablets and a production method thereof. The preparation method comprises the following steps of: removing skin and flesh of fresh wood frog; boiling with water to remove fat; drying and then crushing into wood frog bone powder of over 300 meshes; mixing 45-60 percent by weight of wood frog bone powder, 15-20 percent by weight of calcium carbonate, 5-8 percent by weight of casein phosphopeptide (CPP), 3-5 percent by weight of zinc gluconate, 0.2-0.5 percent by weight of vitamin D3 and a proper amount of auxiliary materials such as mannitol, microcrystalline cellulose and magnesium stearate; and tabletting. The product has the effects of promoting bone growth, enhancing bone density, increasing muscle flexibility and effectively preventing osteoporosis and is particularly suitable for calcium deficiency.
US20120122807 Cardiac Glycoside Analogs in Combination with Emodin for Cancer Therapy A method and medicine for treating leukemia or other cancer includes administering to a patient diagnosed with leukemia or other cancer a treatment regimen that includes periodic doses of a combination of emodin and digoxin.
WO2014080997A1 Anti-midkine aptamer and applications thereof The present invention provides an aptamer, which is capable of forming a potential secondary structure represented by formula (I), that binds to midkine (in the formula: X1, X2, X5 and X6 are each the same or different, and represent a bond, or one or two nucleotides selected from a group comprising A, G, C, U and T; X1 and X6, and X2 and X5 each form a Watson-Crick base pair; and X3 and X4 are each the same or different, and represent a nucleotide selected from A, G, C, U and T).
CN103655685A Preparation method of external medicine for treating hand desquamation The invention discloses a preparation method of an external medicine for treating hand desquamation, which comprises the following steps: (a) fetching 40-60g of liquoric root, putting the liquoric root into 80-150ml of alcohol and soaking for 48 hours; (b) filtering the liquid medicine after being soaked in the step (a) to remove residue; and (c) adding 80-150ml of glycerin into the filtered liquid medicine, and sufficiently stirring and mixing. The preparation method disclosed by the invention is reasonable in formula and convenient to take, prevents toxic and side effects, and can effectively treat hand desquamation to eliminate the paint of a patient.
EP2566861A1 Modulators of fatty acid amide hydrolase 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4-chloro-pyridin-3-yl)-amide is described, which is useful as a FAAH modulator. 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4-chloro-pyridin-3-yl)-amide may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). A method of synthesizing 4- (2,2-difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4- chloro-pyridin-3-yl)-amide is also disclosed.
CN1593414A Powder inhalation of tiotropium bromide capsule type and its preparation method The invention relates to a powder inhalation of tiotropium bromide capsule type and its preparation method, wherein the powder inhalation is prepared from tiotropium bromide drug carrying ultra-fine powder and excipient, through the method of spray-drying. The invention realizes fine pouring properties and and low moisture leading property.
US20090018088 Treating cancer with cardiac glycosides The invention provides methods to treat cancer with cardiac glycosides.
WO2004040302A8 REGULATION OF INTERACTION BETWEEN RAPL AND Rap1 It is considered that the disruption of the function of Rap1 as an integrin adhesion regulatory molecule would closely relate to the pathological conditions of immune diseases such as inflammation, allergy, autoimmune disease, cancer immunity and transplantation immunity. Thus, it is expected that the clarification of the integrin adhesion regulatory mechanism by Rap1 contributes to the understanding of the pathological conditions of these immune diseases and the development of therapies therefor. p30 is identified as a molecule relating to the integrin adhesion regulation by Rap1. It is found out that p30 binds to Rap1 and thus controls its function. Use of this finding makes it possible to develop an inhibitor of the binding of p30 to Rap1, develop remedies for inflammation, allergy, autoimmune disease, cancer immunity, transplantation immunity, etc. and, in its turn, clarify the regulatory mechanism.
EP1513546A1 Compositions for therapeutic use comprising a vitamin, a metal salt and insulin or a growth hormone A composition having a variety of therapeutic and cosmetic uses comprises: (i) a vitamin; (ii) a metal salt that provides metal ions in vivo; and (iii) insulin or a growth hormone. Such a composition may be used to treat, for example, genetic disorders, skin diseases, cancer and viral infections.
EP2450352A1 Prophylactic or therapeutic agent for cancer A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-α modulator, and is useful as a prophylactic or therapeutic agent for cancer.
CN103479807A Brain protecting composition as well as preparation method and application thereof The invention discloses brain protecting composition. The brain protecting composition is prepared from the following raw materials in parts by weight: 2-9 parts of sumac extract, 1-7 parts of grape seed extract, 1-5 parts of ginkgo leaf extract, 1-3 parts of alpha-lipoic acid, 1-3 parts of N-acetyl-L-tyrosine and 1 part of lecithin. The invention further discloses a preparation method and application of the brain protecting composition. The brain protecting composition combines the sumac extract, the grape seed extract, the ginkgo leaf extract, the alpha-lipoic acid, the N-acetyl-L-tyrosine and the lecithin for use, so that the brain protecting composition has a significant brain protecting effect, can be used for treating and/or preventing brain damage caused by focal cerebral ischemia, and has a good prospect.
US20120121516 Emulsion Activatable by Ultrasounds and Method for Producing Same The invention relates to an emulsion that can be activated by ultrasounds, comprising, in an emulsion in an aqueous solution, microparticles having a diameter of less than 10 μm and containing an active agent and a gaseous precursor in a liquid form, encapsulated by a first emulsifier. The microparticles contain nanoparticles smaller than 1 μm, in an emulsion in the gaseous precursor, each nanoparticle comprising an inner liquid that contains the active agent and is encapsulated by a second emulsifier.
WO2011041938A1 Composition comprising benzoic acid in combination with organic acid preservatives as active components and use thereof The present invention provides the use of low dose benzoic acid and/or a sodium salt thereof in combination with one or more organic acid preservatives used as active components in the manufacture of the compositions for vagina. The inhibition of the compositions on vaginal normal lactobacilli is weaker, while the inhibition of the compositions on vaginal fungi and/or vaginal pathogenic lactobacilli is stronger. The organic acid preservatives are selected from dehydroacetic acid and/or a sodium salt thereof, propanoic acid and/or salts thereof, sorbic acid and/or salts thereof. The compositions of the present invention are particularly useful in inhibiting vaginal fungi, and/or inhibiting vaginal pathogenic lactobacilli, and/or facilitating vaginal normal lactobacilli, and/or maintaining normal vaginal acidity, and/or regulating vaginal microecosystem, and/or regulating vaginal microorganisms, and/or selectively decontaminating vagina.
CN102512431A Application of centella asiatica triterpenoid component to preparing anti-craniocerebral injury product The invention relates to application of a centella asiatica triterpenoid component to preparing an anti-craniocerebral injury product, namely new application of asiaticoside and aglycone asiaic acid thereof, madecassoside and aglycone madecassoside thereof to preparation of medicaments for treating craniocerebral trauma and sequelae thereof. As proved by animal tests, the asiaticoside and the aglycone asiaic acid thereof, the madecassoside and the aglycone madecassoside thereof show obvious bioactivity and strong pharmacological action, and has the effects of treating the craniocerebral trauma and preventing and relieving cerebral trauma sequelae (such as depression and dementia). The component has stable property and rich raw material resource, is low in cost, safe and low-toxicity and provides a new medicinal source for preventing, diagnosing, detecting, protecting, treating and researching the craniocerebral trauma and preventing and relieving direct related diseases such as craniocerebral trauma sequelae and the like; and the component has a simple preparation process and high yield, is suitable for industrial production, is easy to promote and apply and has a significant value on developing and utilizing medicinal plant resources of China.
WO2006088790A3 Use of chlorine dioxide for the treatment of onychomycosis (nail fungus) A method for treating nail fungus by soaking the infected nail(s) in a dilute solution of chlorine dioxide in water.
US7842311 for oral dosage; for treatment of pain; sustained release Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact.
CN101851220A Isoprene flavonoid compound and application thereof The invention relates to a novel isoprene flavonoid compound represented by a structural formula selected from the following group and a medicinal composition containing at least one such compound.
CN103301091A Gastrodin double-pulse drug-release preparation The invention relates to the field of pharmaceutical preparation, and in particular relates to a gastrodin double-pulse drug-release preparation. The preparation consists of quick release pellets and slow-release pellets, wherein the quick release pellets consist of gastrodin quick release pellet cores and quick release layers, and the slow-release pellets consist of gastrodin slow-release pellet cores, swelling layers and time-lag layers. By utilizing the gastrodin double-pulse drug-release preparation provided by the invention, the application range of water-soluble medicinal gastrodin with short half-life period is widened in the insomnia treatment field, and the pulse drug release of the double-pulse drug-release preparation can be realized in two key time points at fixed times in an insomnia process; moreover, problems of difficulty in sleeping and early awakening of insomnia patients can be solved, and the sleeping time and quality are ensured.
WO2009093253A3 Compositions and methods for modulating vascular endothelial growth factor c (vegf-c) expression The present invention relates to compounds and methods for inhibiting the expression of vascular endothelial growth factor-C (VEGF-C) in a target cell. Particularly, the present invention relates to antisense polynucleotides complementary to a lens epithelium-derived growth factor (LEDGF/p75) mRNA and uses thereof for inhibiting tumor progression and tumor metastasis. The present invention further relates to uses of LEDGF/p75 polypeptide or a nucleic acid encoding same for treating endothelial cell related conditions, particularly inflammation and edema.
CN100998650A Use of cinnamonum cassia for treating diabetes, its products and preparing method An application of cinnamon bark containing methylhydroxy chalcone polymer in preparing medicines, health-care products, or food for preventing and treating diabetes is disclosed.
EP2419423A1 Fluoro substituted pyrimidine compounds as jak3 inhibitors The present invention relates to compounds of formula (I) wherein AA, R2 to R7 and X1 to X3 have the meaning as cited in the description and the claims. Said compounds are useful as selective inhibitors of JAK3 over JAK2 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
US20110033503 Dressing compositions and methods Described is a spray-on hydrogel comprising water-soluble PEG polymers that cross-link in situ to form a hydrogel such that the cross-links are reversible. The hydrogel can be useful as a drug delivery composition, wound dressing or surgery adjuvant. Polyethylene glycol polymer and cross-linker solutions are sprayed simultaneously through a common orifice. Cross-linking via formation of thioether or disulfide bonds is initiated upon mixing, providing rapid gelation. The hydrogel components can be derivatized with RGD peptides or analogs thereof to promote retention in/on a body compartment such as the skin, surface of the eye, or a mucosa such as the vaginal mucosa. The cross-links are reversed using a reducing solution enabling easy removal of the hydrogel by dissolution. Processes for preparation of the cross-linker, RGD derivatized PEG and RGD-linked agents are also disclosed.
US7758883 first layer has polyvinyl alcohol, polyvinyl acetate, and polyvinyl pyrrolidone; aqueous layer over the first layer;and a layer of a phospholipid (e.g., lecithin) over the aqueous layer; for treating dry eye syndrome An artificial tear film over the surface of an eye having a first layer in direct contact with the ocular surface, an aqueous layer over the first layer, and a layer of a phospholipid over the aqueous layer. The first layer has polyvinyl alcohol, polyvinyl acetate, and polyvinyl pyrrolidone. The phospholipid is derived from Amisol® Clear. The artificial tear film is effective in significantly prolonging the tear break up time in patients with dry eye syndrome.
US20050232915 Matrix metalloproteinase inhibitors in combination with hypothermia and/or radiotherapy for the treatment of cancer The invention provides a method of treating cancer in a subject in need of such treatment which comprises: radio-therapy, or cytotoxic therapy in combination with heat shock, and further comprises administering to the subject an effective amount of a matrix metalloproteinase.
CN101890031B External medicinal composition for treating skin ulcer and preparation method thereof The invention discloses an external medicinal composition for treating skin ulcers (bedsores, burn ulcers and crural region ulcers) and a preparation method thereof, and belongs to the technical field of medicaments. The compound refined white sugar formulation of the composition of the invention is a medicinal composition which is prepared by mixing the medicinal active ingredients such as refined white sugar, neomycin sulfate (or kanamycin sulfate or povidone iodine) and a medicinal diluent or a carrier. In a skin external medicine administration form, the formulation of the composition canbe powder or ointment which is used for treating the skin ulcers such as the bedsores, the burn ulcers, the crural region ulcers and the like.
CN103083351A Pharmaceutical composite preparation of water-soluble vitamin for injection and fat-soluble vitamin injection The invention discloses a pharmaceutical composite preparation of a water-soluble vitamin for injection and a fat-soluble vitamin injection, which belongs to the technical field of medicines. The pharmaceutical composite preparation is prepared from the water-soluble vitamin for injection and the fat-soluble vitamin injection (II). Investigation is carried out on solubility, quality stability of a hydrolysis solution and clinical effects of the preparation at different temperatures, and results show that the pharmaceutical composite preparation has better solubility, stable quality and accurate clinical effects and has obvious advantages in clinical usage.
US20080145339 Modified rolling circle initiator protein for use as therapeutic tool in suppression of viral replication and disorders AAV Rep78 mutants comprising a modified AAV Rep78 protein that possesses different biochemical and biological functions as compared to the wild-type AAV Rep78 protein are disclosed. Particularly, the AAV Rep78 mutants that bind to at least one of a papillomavirus DNA or an AAV DNA or an oncogene or HIV DNA differently as compared to the wild-type AAV Rep78 protein, assays to select such mutants, and pharmaceutical compositions containing the AAV Rep78 mutants are disclosed. The present invention further discloses DNA sequences encoding at least one AAV Rep78 mutant that possesses different biochemical and biological functions as compared to the wild-type AAV Rep78 protein and pharmaceutical compositions comprising the DNA sequences. The present invention additionally is directed to a method of inhibiting papillomavirus associated diseases comprising administering pharmaceutical compositions containing AAV Rep78 mutants or the DNA sequences encoding the mutants. Also discloses are DNA sequences comprising the full length AAV genome modified to where the AAV Rep78 protein is replaced with an AAV Rep mutant that binds weakly or not at all to a papillomavirus DNA or an AAV DNA or both differently as compared to the wild-type AAV Rep78 protein and its use in producing recombinant AAV at increased levels production over wild-type levels of production. Further disclosed is a method of inhibiting papillomavirus-associated diseases, cancer, and HIV-associated diseases comprising administering a pharmaceutical composition comprising a wild-type AAV Rep78 or a mutant thereof to a patient afflicted with a papillomavirus-associated disease, cancer, or HIV-associated diseases. Particularly, useful in treating papillomavirus-associated diseases are the AAV Rep78 or mutant thereof that binds to nucleotides 14-56 of p97 of HPV-16 and inhibits expression of HPV oncoproteins. An AAV Rep78 regulation element of a DNA sequence comprising about nucleotides 14-56 of the nucleotide sequence of FIG. 2 and an AAV Rep78 regulatable promoter comprising the regulation element and a promoter sequence except for the HPV-16 p97 promoter.
CN1813805A Dral solid formulation and its preparing method The present invention discloses a kind of six spirits oral solid preparation, including six spirits tablet preparation and six spirits capsule preparation (hard capsule preparation and soft capsule preparation). Its tablet core or capsule contents can be made up by using 0.5-80% of six spirits pill powder and 20-99.5% of auxiliary material. It has the functions of clearing away heat and toxic material, relieving inflammation and stopping pain, can be used for mainly curing the diseases of sore-throat, laryngopharyngitis, acute throat trouble, tonsillitis, furuncle in children, large carbuncle, acute mastitis, innominate inflammatory swelling, and can obtain good therapeutic effect for curing the diseases of herpes zoster, phlebitis, leukemia, tumor in digestive tract and mammitis, etc.
CN102503930A 3, 4, 5-tri-substituted aminothiopene chemical compound and preparation and application thereof The invention provides a 3, 4, 5-tri-substituted aminothiopene chemical compound. Substituted benzene is used as a raw material to produce derivatives of the 3, 4, 5-tri-substituted aminothiopene chemical compound after being subjected to Friedel-Crafts acylation reaction, Knoevenagel condensation, cyclization, hydrolysis reaction and condensation. The chemical compound and salt thereof have evident effect on blocking interaction of p53-MDM2 (murine double minute 2) and evident inhibitory activity for proliferation in vitro of tumor cells according to demonstration of pharmacological experiments, and the IC 50 (half maximal inhibitory concentration) can reach the mu M level. The 3, 4, 5-tri-substituted aminothipene is reasonable in design, simple and convenient in preparation method and applicable to practical use and can be applied to preparation of antineoplastic medicines, raw materials for the 3, 4, 5-tri-substituted aminothipene are rich in sources, reaction conditions are mild and yield of each step of the preparation method is high. The structural formula of the 3, 4, 5-tri-substituted aminothipene is shown.
CN101574416A Heat-clearing Ganoderma lucidum polysaccharides health-care capsule The invention discloses a heat-clearing Ganoderma lucidum polysaccharides health-care capsule. The components and weight content of the health-care product are: 20 to 50 percent of Ganoderma lucidum polysaccharides, 5 to 60 percent of Ganoderma lucidum polysaccharides byproducts, 3 to 25 percent of pachymaran, 10 to 50 percent of pachymaran byproducts, and 4 to 10 percent of goldthread roots. The heat-clearing health-care product containing the Ganoderma lucidum polysaccharides as main components can be preserved at normal temperature, has the efficacy of the Ganoderma lucidum polysaccharides in enhancing the immunologic function of human body, and also has the efficacy in facilitating absorption and causing no internal heat.
CN101099827A 'Bailing' antiphlogistic ointment The invention is concerned with the antiphlogistin, it is: white petroleum jelly is as substrate, adds into sulfanilamide crystal powder, borneol powder, catechu-tree powder, qingdai powder, lily root powder, which have dramatic curative effect with burn, scalding, abscess, etc, especially with fast acesodyne and without scar.
US7507839 e,g, 1,5-bis(5-acetyl-4,7-dimethoxybenzofuran-6-yloxy)pentane;potassium channel modulator; antiinflammatory agent, autoimmune diseases; immunosuppressant; multiple sclerosis, rejection of foreign organ transplants Various divalent ligands based on khellinone derivatives are described. These derivatives can be useful in the modulation of potassium channel activity in cells, including among others Kv1.3 channels found in T-cells. The compounds may also be useful in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis.
WO2010007181A2 New salt forms of an aminoindan derivative The present invention relates generally to novel salt forms of R-(+)-N-propargyl-1- aminoindan ( i.e .rasagiline base), to a compound of formula Ia, to processes for their preparation and isolation, and to pharmaceutical compositions comprising the same.
US20070299109 Dimeric Compounds Of Piperidine, Piperazine Or Morpholine Or Their 7-Membered Analogs Suitable For The Treatment Of Neurodegenerative Disorders Formula (I″), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof.
WO2011128395A1 N- substituted 3-amino 4 - ( pyrrolidine - 1 - carbonyl) pyrrolidine and its derivatives for use in the treatment of metabolic disorders The present invention is directed to therapeutic compounds which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes. The compounds may also inhibit DPP-IV enzyme activity.
US6858018 Iontophoretic devices Iontophoretic devices for the delivery of N-phenyl-N-(4-piperidinyl)amide esters are provided. The N-phenyl-N-(4-piperidinyl)amide esters are compounds of the 1. A reservoir comprising a matrix material and, distributed in said matrix material, a pharmaceutically acceptable amount of at least one compound selected from compounds of the formula (I) wherein: X is a member selected from the group consisting of alkoxy-carbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxy-carbonyl-lower alkyl, and (C1-2)alkoxy-(C1-2)alkoxy-carbonyl-lower alkyl; Ar is a member selected from the group consisting of phenyl, and mono-, di- and tri-substituted phenyl, wherein each substituent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl; R is a member selected from the group consisting of lower alkyl, and lower alkoxy-lower alkyl,; R1 is a member selected from the group consisting of hydrogen, lower alkoxy-carbonyl; and R2 is a member selected from the group consisting of hydrogen and methyl; and the optically active and cis-trans isomers thereof, and the acid addition salts, of said compounds and isomers.
US7910770 3-Isopropoxy-7-methoxy-N-(1H-1,2,3,4-tetrazol-5-yl)-1-benzo[b]thiophene-2-carboxamide; autoimmune diseases such as rheumatoid arthritis, immune thrombocytopenia purpura, systemic lupus erythematosus and Crohn's disease The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl ring substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the FcγRIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.
US20080260830 suitable for regeneration, growth stimulation and differentiation of various cells, tissues and organs; growth/differentiation factors (GDFs); regeneration of connective tissue including tendon and/or ligament, periodontal or dental tissue including dental implants, neural tissue and sensory tissues The invention relates to novel biosynthetic growth factor mutants which exhibit improved biological activity.
CA2481876C Inhalation kit comprising inhalable powder of tiotropium The invention relates to a method for the administration of powdered preparations containing tiotropium via inhalation.
US20100076035 Transdermal Drug Delivery using an Osmolyte and Vasoactive Agent A formulation and method for delivery of bioactive substances when applied to, or within, the skin or other exterior region of a mammal. for example, a patient, includes a vasoactive agent; an osmolyte; and an active ingredient. The formulation is sufficiently hygroscopic so as to create a condition of hypertonicity when absorbed by the skin. When the formulation is applied to the skin, the vasoactive agent can be delivered to the dermis so as to contact the vasculature of a patient.
US20110244002 Mesoporous material excipients for poorly aqueous soluble ingredients The present invention encompasses formulations and methods for producing solid dispersions comprising mesoporous materials with poorly aqueous soluble active ingredients. The active ingredient is formed in the amorphous state and entrapped in the nanosized pores of the mesoporous excipients using a co-spray drying process. The pore walls of mesoporous channels stabilize the amorphous form of active ingredient against re-crystallization. The amorphous active ingredient entrapped in mesoporous channels exhibits good stability during extended storage under stress test conditions and possesses significantly enhanced dissolution rates.
US20110065758 Compositions and assays for treatment and diagnosis of helicobacter pylori infection and conditions Methods of diagnosing Helicobacter pylori infection or associated conditions are based in part on the correlation of the presence of a α-L-fucosidase 2 marker with the infection. Methods and compositions for treating or preventing Helicobacter pylori infection or associated conditions are based in part on administering an α-L-fucosidase 2 inhibitor to an infected subject or a subject at risk of developing the infection.
WO2014040228A1 Stabilised amorphous form of agomelatine, a process for its preparation and pharmaceutical compositions containing it The present invention relates to the stabilised amorphous form of the compound of formula (I), to a process for its preparation and also to pharmaceutical compositions or medicaments containing it.
WO2008156012A1 CANCER REMEDY CONTAINING MORTALIN siRNA An siRNA or shRNA the target sequence of which is a base sequence represented by one of SEQ ID NOS:1 to 6. Thus, an anticancer agent using mortalin shRNA can be provided.
CN101254241A Healing composition for treating wart The invention relates to a Xiaoyoukang compound preparation, belonging to the field of medical formula. The inventive compound preparation is prepared from (wt%) concha cypraeae violacae 16-22,voncha ostreae 8-11, hematite 10-16, magnetite 10-16, radix paeoniae rubra8-11, flos lonicerae 8-11, isatis indigotica root 10-16, paris polyphylla 7-10, and astragalus membranaceus 3-7. The preparation method comprises the following steps of washing the above raw materials, soaking in water, decocting, filtering to remove residues, collecting filtrate, and refining to obtain a mixture. The compound preparation had good therapeutic effect on flat wart; and has the advantages of low raw material cost, simple process, no toxic or side effects, high compliance, and easiness for clinic popularization.
US20090227537 Sulfated polysaccharides and uses thereof in medical treatment The invention provides sulfated oxidised regenerated cellulose compounds, sulfated alginates, and the salts and hydrates thereof. The compounds are obtained by sulfation of oxidised regenerated cellulose with sulfur trioxide. The invention also provides pharmaceutical compositions comprising the compounds, in particular compositions for the treatment of medical conditions mediated by a matrix metalloproteinases and anticoagulant pharmaceutical compositions.
WO2012137142A1 Novel salts of raltegravir The present invention provides novel salts of raltegravir, viz., meglumine salt, erbumine salt, ammonium salt, tris salt and L-arginine salt of raltegravir and processes for their preparation.
CN103183598A 1,2-diaryl-2-propenyl-1-ketone compounds and use thereof The invention belongs to the technical field of medicines, relates to 1,2-diaryl-2-propenyl-1-ketone compounds and use thereof, and particularly relates to the compounds and application thereof as a tumor cell proliferation inhibitor and a tumor vascular disrupting agent in field of preparation of anti-cancer medicines. The compounds of the present invention can be represented by a structural formula in the specification, wherein R1-R8 are defined as the specification.
WO2008084324A1 Naphthyridinone compound This invention relates to a compound of formula (I) (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the compound or a salt thereof, and its use as a medicament for the treatment of schizophrenia, bipolar disorder, or other central nervous system disorders.
US20090048324 Alternate morpheein forms of allosteric proteins as a target for the development of bioactive molecules A composition having an agent adapted to affect a multimeric protein by binding to a binding site of the multimeric protein and thereby affecting an equilibrium of units, wherein the multimeric protein has an assembly having a plurality of said units, wherein each of the units has a first complementary surface and a second complementary surface and wherein the first complementary surface of one unit is associated with the second complementary surface of another unit, provided that the assembly is at least one of different quaternary isoforms on a condition that in the multimeric protein (1) a structure of each of the units determines a structure of the different quaternary isoforms, (2) the units are in the equilibrium and (3) the structure of the different quaternary isoforms influences a function of the multimeric protein.
CN101766596A Solid preparation with dextro-oxiracetam as active component The invention provides a solid preparation with dextro-oxiracetam as an active component, relating to an oral preparation of the dextro-oxiracetam that is an annular derivant of hydroxyl aminobutyric acid (GABOB). The solid preparation contains the dextro-oxiracetam or salt or a purified hydrate thereof shown in the following structure; the chemical name is oxiracetam 4-hydroxy-pyrrolidine-2-ketone-1-acetamide; and the oral solid preparation is prepared by the dextro-oxiracetam and accessories that can be accepted in terms of pharmacy through the preparation technology. The dextro-oxiracetam which uses a single optical isomer can achieve better curative effect and milder toxic/side-effects than a racemate. The solid preparation of the dextro-oxiracetam is safe as well as effective, can be controlled and has stable quality.
CN103736093A Medicinal preparation comprising mizolastine and steroid The invention relates to a medicinal product or a preparation which comprises mizolastine or pharmaceutically-acceptable salts, solvates or physiologically-functional derivatives thereof, and a steroid or pharmaceutically-acceptable salts, solvates or physiologically-functional derivatives thereof. In particular, the product or the preparation is suitable for an intranasal or ophthalmic administration form.
US7018995 Carbonate and carbamate modified forms of glucocorticoids Carbonates and carbamates of the formula and related steroid carbonates and carbamates are disclosed. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.
CN101584665B Cefotiam hydrochloride medicament composition sterile powder injection and preparation method thereof The present invention discloses a cefotiam hydrochloride medicament composition sterile powder injection, including 500 to 600 weight shares of cefotiam hydrochloride and 110 to 150 weight shares of anhydrous sodium carbonate. The cefotiam hydrochloride medicament composition sterile powder injection has advantages of a good stability and a high purity. The invention also discloses a method for preparing the cefotiam hydrochloride medicament composition sterile powder injection, including steps of weighing the cefotiam hydrochloride and the anhydrous sodium carbonate according to the formula amount separately and mixing them in a sterile container uniformly. The method is simple, and the cefotiam hydrochloride prepared by the above method has a good stability.
US8377961 Cyclic-alkylamine derivatives as inhibitors of the interaction between MDM2 and P53 The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R1, R2, R3, R4, R5, R6, R7, Q, Y and Z have defined meanings.
US20080207685 Heterocyclic Compounds As Modulators Of Peroxisome Proliferator Activated Receptors, Useful For The Treatment And/Or Prevention Of Disorders Modulated By A Ppar The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
WO2011086347A1 Pyrrolidine iminosugars used in the treatment of cystic fibrosis A compound of formula (I) wherein: R1 is selected from H; linear or branched, substituted or unsubstituted alkyl, alkenyl, alkynyl and aralkyl and wherein the optional substitution may be with one or more groups independently selected from: -OH; -F; -Cl; -Br; -I; -NH2; alkylamino; dialkylamino; linear or branched alkyl, alkenyl, alkynyl and aralkyl; aryl; heteroaryl; linear or branched alkoxy; aryloxy; aralkoxy; -(alkylene)oxy(alkyl); -CN; -NO2; - COOH; -COO(alkyl); -COO(aryl); -C(O)NH(alkyl); -C(O)NH(aryl); sulfonyl; alkylsulfonyl; arylsulfonyl; sulfamoyl; alkylsulfamoyl; alkylthio; alkylsulfonamide; arylsulfonamide; -NHNH2; and -NHOH; or a bioisostere, pharmaceutically acceptable salt or derivative thereof, finds application in the treatment of cystic fibrosis.
EP2012792A1 Use of a compound inducing an increase of free serotonin rate in the body, for preparing a medicine for treating skeletal muscle degeneration The invention concerns the use of a compound inducing an increase of free serotonin rate in the body, for preparing a medicine for treating conditions corresponding to muscular degeneration of skeletal muscles such as muscular myopathies of genetic origin, and in particular Duchenne's myopathy or cachexias.
CN103102358A Cephalosporin compound, crystal thereof, and preparation method and application thereof The invention relates to a (6R, 7R)-3-[(acetyloxy) methyl]-7-[alpha-(N, N'-dicyclohexyl amidine thio)-acetylamino]-8-oxo-5-thia-1-azabicyclo [4, 2, 0]-oct-2-ene-2-carboxylic acid, a crystal thereof, and a preparation method and application thereof. Under alkaline conditions, 7-ACA reacts with bromoacetyl bromide to obtain a 7-bromo acetamino-3-[(acetyloxy) methyl]-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2 formic acid intermediate A; and the intermediate A reacts with N, N '- dicyclohexyl thiourea to obtain the compound provided by the invention. The compound is further refined to obtain the crystal with high purity and good stability of the compound provided by the invention. The compound and the crystal thereof have antibacterial effect on Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae and Enterococcus faecalis, and are potential antimicrobial drugs with promising application prospect.
EP1560572A1 Topical parasiticide formulations and methods of treatment Aqueous micellar formulations for topical administration of benzimidazoles or salicylanilides with macrocyclic lactones to livestock for the control of endoand ecto-parasites, comprising a first active agent selected from water insoluble benzimidazoles, salicylanilides and active derivatives or salts thereof, in combination with a second active agent selected from macrocyclic lactones or active derivatives or salts thereof, and also comprising, per litre of formulation: from about 100 to about 400g veterinary acceptable surfactant(s); from about 200 to about 750g veterinary acceptable water-miscible solvent(s); and from about 50 to about 350g water, as well as methods for dosing livestock with such formulations, and methods for controlling and/or preventing diseases or parasite infection in livestock.
CA2304950C Acidic aqueous chlorite teat dip providing shelf life, sanitizing capacity and tissue protection The mastitis control teat dip composition of the invention provides rapid initial kill, a useful highly pseudoplastic rheology, a barrier/film-forming capacity, a unique antimicrobial composition that is stable over an extended period of time, and unexpected long term microbial control when compared to the prior art materials disclosed in patents and used in the marketplace. The compositions of the invention are made by combining an aqueous thickened liquid composition containing the organic components which can be combined with a simple aqueous solution of a salt of chlorous acid, preferably an alkali metal chlorite. The materials can be combined, blended into a smooth viscous material and can be immediately contacted with the target animals. The compositions of the invention provide rapid initial kill, consistent long term kill and chemical and rheological stability.
US20110046226 Pharmaceutical compositions for prevention of overdose or abuse The invention relates to pharmaceutical compositions comprised of a chemical moiety attached to an active agent in a manner that substantially decreases the potential of the active agent to cause overdose or to be abused. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent.
EP0990002B1 Dextran derivatives, preparation method and applications as medicine with specific biological action The invention concerns dextran derivatives, their applications as medicines with specific biological action, and their preparation method. Said derivatives correspond to the general formula DMCaBbSUcSd, in which: D represents a polysaccharide chain, preferably consisting of sequences of glucoside units, MC represents methylcarboxylate groups, B represents carboxymethylbenzylamide groups, Su represents sulphate groups, S represents sulphonate groups, a, b, c and d represent the degree of substitution (ds), respectively in groups MC, B, Su and S; a being equal to 0 or >/=0.3, b being equal to 0 or >/=0.1, c being equal to 0 or >/=0.1 and d being equal to 0 or a and/or b are not equal to 0, said products having homogeneity of chain size distribution, illustrated by a gaussian elution profile symmetrical in high performance steric exclusion chromatography, and homogeneity in the distribution of charged chemical groups, illustrated by an elution profile with a single symmetrical peak in low pressure ion-exchange chromatography.
WO2007116960A1 Oxazolidinone derivative having carbocyclic ring Disclosed is a novel oxazolidinone derivative represented by the formula (I). Also disclosed is an antibacterial agent comprising the derivative, wherein the ring A represents an at least 7-membered monocyclic carbocyclic ring which may be substituted and whose ring may be fused; X1 represents a heteroatom-containing group selected from the group consisting of -O-, -S-, -NR2-, -CO-, -CS-, -CONR3-, -NR4CO-, -SO2NR5- and -NR6SO2- (wherein R2 to R6 independently represent a hydrogen, a lower alkyl, or a lower alkoxycarbonyl) or a lower alkylene or alkenylene which may contain the heteroatom-containing group; the ring B represents a carbocyclic or heterocyclic ring which may be substituted; and R1 represents a hydrogen or an organic residue which can bind to position-5 of an oxazolidinone ring in an oxazolidinone-type antibacterial agent (wherein a combination of -CH2O- as X1 and a hydroxymethylene which may be substituted as R1 is excluded).
US20060251751 Sophoridine and its use as an analgesic The present invention relates to use of natural or chemically synthetic sophoridine and its analogues or derivatives as an analgesic. The present invention further related to pharmaceutical compositions comprising alkaloid compounds having diquinolizidine-like structure selected from the group consisting of sophoridine, sophocarpine, matrine, oxymatrine, malanine, aloperine, sophoramine, and pharmaceutically acceptable salts thereof, and one or more pharmaceutically acceptable carriers or excipients. The pharmaceutical compositions of the present invention can be used for eliminating or alleviating acute or chronic pain without suffering from the undesirable tolerance and addiction with continued usage.
CN1839874A Water-soluble vitamin formulation containing sodium calcium ethylene diamine tetracetate for injection and its preparation method The invention discloses a water-soluble vitamin formulation containing sodium calcium ethylene diamine tetracetate for injection and its preparation method, wherein each 10ml of the preparation comprises vitamin B1 2.8-3.2mg, biotin 55-65mug, vitamin B2 3.0-4.0mg, folic acid 0.35-0.45mg, nicotinamide 35-45mg, vitamin B12 4.5-5.5mug, vitamin B6 3.5-4.5mg, glycine 290-310mg, sodium pantothenate 12-16mg, methyl-p-hydroxybenzoate 0.4-0.6mg, vitamin C 90-110mg, EDTA-Ca 0.4-0.6mg. The preparing process consists of the steps of batching, degerming and filtering, loading, freeze-drying and packaging.
US20100151048 For therapy of psoriasis, eczema, ichthyosis, pruritus, dryness and dermatitis, which may cause skin to crack, chap or chafe A composition and method for the prevention and therapeutic treatment of skin conditions and disorders are disclosed. The composition and method of the invention are particularly directed to the treatment and prevention of dermal irritations. These irritations include, for example, psoriasis, eczema, ichthyosis, pruritus, dryness and dermatitis, which may cause skin to crack, chap or chafe. The composition and method are particularly useful in treating and preventing diaper dermatitis. A therapeutic composition according to the invention includes an agent, which is an enzyme constituent, promoting the synthesis of collagen and the reproduction of cells, particularly skin cells. Such therapeutic agents include, for example, zinc oxide. This agent is generally nonprescription and capable of effectively preventing and treating diaper dermatitis through local or topical application. Therapeutic compositions according to the invention also include both natural and synthetic components, which aid in application, use and treatment.
WO2011161615A1 5-lipoxygenase inhibitors The present invention relates to pyrazole derivatives of formula 1 and to process as for their synthesis as 5-lipoxygenase (5-LO) inhibitors. The present invention also relates to pharmacological compositions containing these pyrazole derivatives, as well as, methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, Type I diabetes, psoriasis, allograft rejection, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, allergic rhinitis and other inflammatory and/or autoimmune disorders.
US20090062266 7-methoxy-2-methyl-N-[[(5S)-[3-[3-fluoro-4-(piperazin-1-yl)phenyl]-2-oxo-5-oxazolidinylmethyl]-3-quinolinecarboxamide, useful for the treatment of grampositive and some gramnegative bacterial infections, with a weak monoamine oxidase inhibitory activity The invention provides new oxazolidinone compounds of formula (I) wherein A is certain heterocycles optionally substituted; R1, R2, R3 and R4 are independently selected from —H and halogen; X is selected from O, S, NR9 and CR9R10; R9 and R10 having different meanings; Y is selected from O, S, SO, SO2, NO, NR12 and CR12R13; R12 and R13 having different meanings. It also provides different processes for the preparation of such compounds. Oxazolidinone compounds of formula (I) are active against Gram-positive and some Gram-negative human and veterinary pathogens with a weak monoamine oxidase (MAO) inhibitory activity. They are useful for the treatment of bacterial infections.
CN1789250A Optical antimer of a group of nitro imidazole derivatives, preparation method and uses thereof The invention relates to a process for preparing optical enantiomers of nitroimidazole derivatives and the use of these compounds in preparing anti anaerobe medicaments.
WO2009138176A1 Substituted imidazo- and triazolopyrimidines, imidazo- and pyrazolopyrazines and imidazotriazines as gsk3beta-inhibitors The invention relates to substituted imidazo- and triazolopyrimidines, imidazo- and pyrazolopyrazines and imidazotriazines and to methods for the production thereof, and also to the use thereof for the production of pharmaceuticals for the treatment and/or prophylaxis of diseases; in particular of hematologic diseases, preferably of leucopenia and neutropenia. Formula (I) in which A stands for a group of formula (II), (III), (IV), (V) or (VI) wherein #1 means the binding site for the heterocycle substituted with R1, #2 means the binding site of the carbon atom to which R13 is bonded, #3 means the binding site of the carbon atom to which R4 is bonded.
WO2006091112A1 Compositions for the delivery of rna interference molecules and methods for their use The present invention provides compositions for the treatment and/or prevention of a disorder in a mammal by means of RNA interference, together with methods for the use of such compositions. The inventive compositions comprise a small interfering nucleic acid molecule (siNA) that suppresses expression of a target gene within the target cell, or a genetic construct that expresses such a siNA, wherein the target gene is CXCR4, SDF-1 and/or HCLCA1.
EP1561751A1 Fluorene carboxylic acid esters, methods for the production thereof, and use of the same as pharmaceuticals Esters (I) of fluorene-9-carboxylic acid with a bicyclic nitrogen heterocycle are new. - Esters, of formula (I), of fluorene-9-carboxylic acid with a bicyclic nitrogen heterocycle are new. - A = -CH2CH2-, -CH=CH- or oxiranyl; - X- = monovalent anion; - R = hydrogen, hydroxy, Me, Et, trifluoromethyl, difluoromethyl or fluoro; - R1 and R2 = 1-5C alkyl, optionally substituted by 3-6C cycloalkyl, hydroxy or halo, or both together form a 3-5C alkylene bridge; and - R3, R4, R3' and R4' = hydrogen, 1-4C alkyl or alkoxy, trifluoromethyl, difluoromethyl, cyano, nitro or halo. - Independent claims are also included for: - (1) Intermediates of formula (IV) and their acid addition salts; and - (2) Use of intermediates (II), or their acid addition salts, in the preparation of (I). - ACTIVITY - Antiasthmatic; Cardiant; Antiarrhythmic; Uropathic; Gynecological; Spasmolytic. - No biological data available. - MECHANISM OF ACTION - Anticholinergic; - Compounds (I) are antagonists of muscarinic receptors, subtype 3, generally with affinity (Ki) below 10 nM.
CN102485213A Irinotecan liposome and preparation method thereof The invention belongs to the technical field of medicine and relates to irinotecan liposome and a preparation method thereof. The method can control ethanol content in liposome during a preparation process and ensure no substantial influence of residual ethanol on liposome property in the preparation process. The invention employs improved ethanol injection method to prepare irinotecan liposome, and a membrane material comprises phospholipid or / and other components. The method comprises steps of: preparing a hydrating medium at 45-75 DEG C and insulating for standby; dissolving lipid phase with ethanol, including absolute ethyl alcohol, in a volume less than 10% of a final volume of a preparation at 45-75 DEG C; adding the hydrating medium into the lipid phase at a certain speed; stirring and dispersing to reduce grain size and obtain a blank liposome; and loading according to a gradient method. The invention can effectively control residual ethanol amount during the preparation process, and physical and chemical properties of the liposome have no significant change.
US20090192111 miR-124 Regulated Genes and Pathways as Targets for Therapeutic Intervention The present invention concerns methods and compositions for identifying genes or genetic pathways modulated by miR-124, using miR-124 to modulate a gene or gene pathway, using this profile in assessing the condition of a patient and/or treating the patient with an appropriate miRNA.
CN101181224B Solid dispersion of entecavir, pharmaceutical composition and preparation method as well as uses thereof The invention relates to a solid dispersion composition technology of an entecavir, which adopts entecavir and poloxamer to form a solid dispersion system, so as to well solve the difficult problem of poor water solubility of entecavir and lead the entecavir to be dissolved out rapidly with high efficiency. The invention is also conductive to the even mixing of the active ingredients of the preparation composition and has important significance for the quality improvement of entecavir preparation. The invention also relates to the preparation of entecavir solid dispersion and the drug application.
CA2177602C N-substituted azabicycloalkane derivatives, their preparation and use Compounds of formula (I) where B, R1, R2, n and A have the meanings given in the description, and their preparation are described. The novel compounds are suitable for the control of diseases.
CN102488694A Perfusion medicament for treating milk cow mastitis and preparation method thereof The invention discloses a perfusion medicament for treating milk cow mastitis and a preparation method thereof. The perfusion medicament is prepared from the following raw materials by weight: 0.9-4.3g of cefquinome sulphate, 0.15-0.25g of prednisolone, 0.5-1.3g of flunixin meglumine, 1-1.5g of glycerin monostearate, 3-8g of Vaseline, 0.05g of ethylparaben and 65-70g of whiteruss. The preparationmethod comprises the following specific steps of: (1) putting one tenth of the liquid paraffin into a burdening tank in a certain weight ratio; (2) adding one third of the liquid paraffin into a heating tank; and (3) putting the rest of the liquid paraffin left after the steps (1) and (2) and auxiliary materials in the step (2) into an emulsifying tank, adding 0.9-4.3g of cefquinome sulfate in a certain weight ratio, and stirring till uniform distribution to obtain the perfusion medicament for treating milk cow mastitis. The perfusion medicament has the advantages of no induction of endotoxemia in a milk cow mastitis treating process, remarkable curative effect on mastitis and freeness from medicament tolerance.
CN101418001B Dipeptidase-IV inhibitor sulfonyl urea derivates The invention belongs to the technical field of medicine, and in particular relates to dipeptidyl peptidase IV inhibitor sulfonylurea derivatives of a general formula (I), pharmaceutically acceptable salts or isomers thereof, wherein R<1>, T<2>, R<3>, R<4>, R<5>, X and Y are as defined in the specification. The invention also relates to methods for preparing the compounds, pharmaceutical compositions containing the compounds, and application of the compounds to the preparation of drugs for the treatment and/or prevention of diabetes, non-insulin-dependent diabetes, hyperglycemia, and insulin resistance.
US20090076156 Use of a noradrenergic agonist, e.g. guanfacine, for the treatment of cognitive disorders The present invention relates to the use of a noradrenergic agonist for the treatment of a patient with a cognitive disorder resulting from acquired brain damage, wherein the cognitive disorder includes, for example, hemi-spatial neglect.
WO2007035954A3 Vaginal tablets comprising misoprostol and methods of making and using the same The present invention is directed to vaginal tablets comprising misoprostol and a pharmaceutically acceptable pH insensitive, hydrophilic cellulose material, wherein the vaginal tablets do not contain a hydrophobic release controlling agent, and wherein the misoprostol and the pharmaceutically acceptable pH insensitive, hydrophilic cellulose material are in a ratio of about 1:50 to about 1:800, and wherein the vaginal tablets do not substantially change the pH of a vaginal tract.
WO2014020101A1 Griseofulvin derivatives The present invention relates to compounds of the following general formula (I), or to a pharmaceutically acceptable salt thereof, as well as to the uses thereof as a drug, in particular in the treatment of cancerous or precancerous hyperproliferative conditions, and to the pharmaceutical compositions containing same.
CN1676521A Kuh-seng ketone and its derivative and the like and use in preparing anti-tumor medicine This invention relates to a kuh-seng ketone and its derivant, and the pharmacy use of its analog. It specifically relates to kuh-seng ketone and its vibrant and analog's use in the anticancer medicine. This invention also explores the new medical use of the kuh-seng ketone and its derivant and analogs.
EP1212068A4 Method of enhancing the efficacy of anti-tumor agents A method for enhancing the effect of anti-tumor agents on solid tumors is provided. The method comprises administering to an individual an anti-tumor agent and a hematocrit elevator. The hematocrit elevator may be administered before or concurrently with the anti-tumor agent.
WO2009148137A1 Nucleic acid capable of controlling degranulation of mast cell Disclosed are: an agent for controlling the degranulation of a mast cell; a diagnostic or therapeutic agent for a disease associated with the control of the degranulation of a mast cell; a method for controlling the degranulation of a mast cell; and a method for the screening of an agent for controlling the degranulation of a mast cell, each of which uses a nucleic acid or the like. The agents and the methods are useful for the diagnosis or treatment of a disease associated with the control of the degranulation of a mast cell.
CN1977841A Method for preparing simvastatin tablet The present invention relates to a preparation method of simvastatine tablet. It is characterized by that it adopts direct tabletting process and film coating process. Said tablet quality is stable and uniform, and its solubility is good.
WO2011158806A1 Process for production of hematopoietic stem cell Disclosed is an agent for amplifying a hematopoietic stem cell and/or a hematopoietic progenitor cell, which is useful as a therapeutic method for various hematopoietic diseases and is also useful for the improvement in the efficiency of gene transfer into a hematopoietic stem cell in a gene therapy. Also disclosed is a process for producing a hematopoietic stem cell and/or a hematopoietic progenitor cell, which is characterized by culturing a hematopoietic stem cell in the presence of a compound represented by formula (I) (wherein R1 to R6 are as defined in the description), a tautomer or pharmaceutically acceptable salt thereof, or a solvate of the compound, the tautomer or the pharmaceutically acceptable salt to amplify the cell.
US20090042855 BENZAMIDE mGluR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
US20100183724 Hydrogel of Chitosan Carboxyalkylamide, Preparation Thereof and Cosmetic and Dermatological Use Thereof The present invention relates to a hydrogel of chitosan carboxyalkylamide, characterised in that it has a pH value close to that of the skin, comprised between 6.5 and 7.2, and in that the chitosan carboxy-alkylamide is constituted by 40 to 90 mole % of D-glucosamine N-carboxyalkylamide units of formula (I) where n represents an integer ranging from 1 to 8, from 60 to 10 mole % of protonated D-glucosamine units, and from 5 to 15 mole % of N-acetyl-D-glucosamine units. The present invention also relates to a dehydration product of such a gel and the cosmetic and/or dermatological utilisation of the gel and the dehydration product.
US8053599 Drug containing (2R)-2-propyloctanoic acid as the active ingredient The present invention relates to a medicament which is useful for neurodegenerative diseases, which comprises about 1 to about 5 equivalents of a basic metal ion based on 1 equivalent of (2R)-2-propyloctanoic acid or a salt thereof, which is supplied from a metal salt of weak acid or a metal hydroxide, and optionally further comprises an additive. The medicament of the present invention is a medicament which a pH of suitable for intravenous administration, is resistant to fluctuations of the pH and is not clouded when it is dissolved in an infusion, and an injection and the like can be prepared therefrom by using any dissolving liquid and/or dilution liquid.
EP1308441B1 2-aminopyridine compounds and use thereof as drugs 2-Aminopyridine compounds of the general formula (I) and salts thereof, exhibiting excellent adenosine receptor (A1, A2a, or A2b receptor) antagonism wherein R1 is cyano, carboxyl, or optionally substituted carbamoyl; R2 is hydrogen, hydroxyl, optionally substituted C¿1-6? alkoxy, an optionally substituted C6-14 aromatic carbocyclic group, or an optionally substituted 5- to 14-membered aromatic heterocyclic group; and R?3 and R4¿ are each independently an optionally substituted C¿6-14? aromatic carbocyclic group, a 5- to 14-membered nonaromatic heterocyclic group, a 5- to 14-membered aromatic heterocyclic group, or the like.
US7232830 Administering to a patient a compound for increasing neuronal metabolism of histamine to a histamine H2 agonist, to stimulate production of adenosine 3*,5*- cyclic phosphate at a level which maintains myelin against self degeneration A method for treatment of neurodegenerative disease conditions stemming from multiple sclerosis, aging, autoimmune diseases and fibromyalgia. A compound effective to increase neuronal metabolism of histamine to a histamine H2 agonist is administered in an amount sufficient to stimulate production of cyclic AMP at a level which is sufficient to maintain myelin against undergoing self-degeneration. The compound is selected from the group consisting of histamine M-methyltransferase, monoamineoxidase-A, monoamineoxidase-A agonists and histamine H3 antagonists. The histamine M-methyltransferase may be administered to increase neuronal metabolism of histamine to tele-methylhistamine, whereas the monoamineoxidase-A or monoamineoxidase-A agonist may be administered so as to increase neuronal metabolism of telemethylhistamine to an H2 agonist. Separately or in conjunction with the others, the histamine H3 antagonist may be administered so as to inhibit metabolism of the telemethylhistamine to an H3 agonist, thereby increasing metabolism of the telemethylhistamine to an H2 agonist. The increased histamine H2 agonist levels reduce demyelination and the symptoms that are associated with these conditions.
CN103110616A Potassium magnesium aspartate freeze-dried powder preparation for injection and preparation method of preparation The invention relates to potassium magnesium aspartate freeze-dried powder preparation for injection. The potassium magnesium aspartate freeze-dried powder preparation for injection is prepared from the following materials in parts by weight: 400-600 parts of potassium aspartate, 400-600 parts of magnesium aspartate and 320-480 parts of lactose. The freeze-dried powder preparation disclosed by the invention has the advantages of being simple in prescription and scientific and reasonable in preparation method, so that the freeze-dried product is more fluffy and porous, thereby remarkably improving the re-dissolution of the freeze-dried powder preparation during the clinical use process; meanwhile, the stability of the preparation is further improved on the condition of low auxiliary material dosage and less categories, so that the medication safety of the patient is ensured.
US20110229561 Extended Release Pharmaceutical Composition Of Entacapone Or Salts Thereof There is provided an extended release pharmaceutical composition comprising from about 200 mg to about 1000 mg of entacapone or salts thereof, optionally with other pharmaceutically acceptable excipients. The invention also provides an extended release pharmaceutical composition comprising triple combination of from about 30 mg to about 300 mg of levodopa, 10 mg to about 100 mg of carbidopa and 200 mg to about 1000 mg of entacapone or salts thereof, optionally with other pharmaceutically acceptable excipients. The invention also relates to process of preparation of such compositions.
CA2214072C Benzo [b] thiophene compounds, intermediates, processes, compositions, and methods The instant invention provides novel benzo[b]thiophene compounds of Formula I (see formula I) intermediates, compositions, pharmaceutical formulations, and methods of use.
US20100056613 Spiroquinone compound and pharmaceutical composition A novel spiroquinone derivative having a high ABCA1 stabilization effect and being useful for prophylactic and/or therapeutic agents for various diseases developing hypo-high density lipoproteinemia is obtained. The novel spiroquinone derivative is a compound represented by the following formula: wherein R1a, R1b, R1c and R1d each represents a hydrogen atom, a halogen atom, an alkyl group which may have a substituent, or an alkoxy group which may have a substituent, and R2a and R2b each represents a hydrogen atom, or an alkyl group which may have a substituent (e.g., a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, and an N-substituted carbamoyl group), the groups R2a and R2b may bond together to form a hydrocarbon ring with an adjacent carbon atom, provided that compounds in which all of the groups R1a, R1b, R1c and R1d are t-butyl groups, and both of the groups R2a and R2b are hydrogen atoms or both of the groups R2a and R2b are methyl groups are excluded; or a pharmacologically acceptable salt thereof.
WO2003012072A3 Monoclonal antibodies to activated erbb family members and methods of use thereof Antibodies which bind to activated members of the erbB, TNF, and IgSF family of receptors and pharmaceutical compositions comprising the same are disclosed. Peptides and mimetics of erbB, TNF, and IgSF receptors and pharmaceutical compositions comprising the same are also described. Methods of using such antibodies, peptides, and mimetics in tumor therapeutic, prophylactic, imaging and diagnosing applications are disclosed.
CN102058748A Method for preparing muscle relaxing and blood circulation stimulating capsules The invention relates to the technical field of medicines, and discloses a method for preparing muscle relaxing and blood circulation stimulating capsules. The method is characterized by comprising the following steps of: crushing safflower, nutgrass galingale rhizome, East Asian tree fern rhizome and Chinese silkvine bark into 80-mesh fine powder, and sieving for later use; performing water precipitation on native copper, Chinese starjasmine stem, common clubmoss herb, herba lycopi, coloed mistletoe herb and suberect spatholobus stem to form an extract, concentrating the extract into thick paste, adding the powder, and adding or not adding a filler; and drying at 60 DEG C, crushing into 80-mesh fine powder, and filling into capsules. The capsules have multiple advantages compared with the conventional tablets.
CN1994352B Use of total glucosides extract of cocklebur fruit in preparation of product for resisting inflammatory reaction The invention relates to an application of xanthostrumarin extractive, wherein said xanthostrumarin extractive comprises diterpene compound, phenolic acid compound and other extractives while their contents are 0.5%-99%, 0.5%-99%, and 0.5%. And the production uses general extraction, separation and purification. The extraction is solvent extraction method; the separation and purification uses solvent extraction method and porous adsorption resin method. The inventive extractive can treat coryza, nasal sinusitis, etc. It has simple production and stable property.
CN102755589A Preparation method of Bifidobacterium microcapsules The invention belongs to the technical field of preparation of probiotic products, and particularly relates to a preparation method of Bifidobacterium microcapsules, which comprises the following steps: 1. preparing a composite bacterial suspension; 2. dissolving a wall material; and 3. preparing the composite microcapsules. The invention provides a novel method for preparing Bifidobacterium powder microcapsules, removes the film-forming reaction of chitosan, and lowers the production cost. According to the invention, the Bifidobacterium is embedded into an enteric material isolate the outside air, so that the Bifidobacterium microcapsules are hardly dissolved in gastric acid and slowly release in the intestinal tract; and after the Bifidobacterium microcapsules are digested by the intestinal tract, the bioavailability is enhanced, and the survival rate is higher than the document report.
CN103393993A Drug for treatment of prostatitis The invention provides a drug for treatment of prostatitis, and the drug comprises the following components: by weight, 8-12 parts of cortex cinnamomi, 6-11 parts of anemarrhena, 10-18 parts of radix astragali, 7-15 parts of achyranthes root, 6-10 parts of rheum officinale, 10-18 parts of saltcake, 8-12 parts of desmodium, 9-12 parts of talcum, 6-12 parts of phellodendron, 8-15 parts of plantain seed and 7-15 parts of rhizoma smilacis glabrae. The drug has the advantages and positive effects of good curative effect, short period, small side effect and low treatment cost.
US20120270783 Rapid opioid detoxification Rapid opioid detoxification procedures are provided which include sedating a patient with an anesthetic agent having a short full recovery period. The patient is administered an opioid antagonist while sedated and can be revived to an ambulatory condition within eight hours of initiating therapy. The described methods for detoxification also include administering a diarrhea suppressant, such as octreotide acetate, to limit this unfortunate side effect of the detoxification.
CN103385860A Fexofenadine hydrochloride orally disintegrating tablets and preparation method thereof The invention belongs to medicine field and relates to an orally disintegrating tablet containing fexofenadine hydrochloride and a preparation method thereof, wherein the orally disintegrating tablet comprises the fexofenadine hydrochloride and an excipient. The excipient comprises a filler, a disintegrating agent, a flavoring agent and a lubricant. The preparation method comprises (1) preparation of a solid dispersion and (2) preparation of the orally disintegrating tablets. The orally disintegrating tablets provided in the invention have a good taste and a rapid disintegration period and overcome an unbearable bitter taste generated without taste modification. In the method, a taste shielding method in the solid dispersion technique and the preparation method of the orally disintegrating tablets are used. The methods are simple in process operations, good in controllability and repeatability and low in production cost.
EP1748792A1 Compositions comprising demethylating agents as enhancers of immunotherapy for the treatment of chronic infections and neoplastic diseases and methods for treating the same The invention concerns compositions comprising a demethylationg agent and an antigen for inducing and enhancing antigen-specific immunity and uses thereof. The invention also concerns methods for enhancing antigen-specific immunity by administrating a demethylating agent.
WO2010097583A1 Esomeprazole potassium polymorph and its preparation The present invention provides a polymorph of esomeprazole potassium termed "Form C", which is in the form of an ethanol solvate. There is also provided processes for preparing Form C of esomeprazole potassium and pharmaceutical compositions comprising it.
WO2011069032A3 Formulations, salts and polymorphs of transnorsertraline and uses thereof Provided herein are pharmaceutical compositions comprising transnorsertraline, salts and polymorphic forms of transnorsertraline, methods of making the compositions, and methods for their use for the treatment of CNS diseases, including depression.
CN101590222A SOD cell repair liquid and preparation method thereof The invention relates to SOD cell repair liquid and a preparation method thereof. The repair liquid contains superoxide dismutase (SOD), aloe juice, hyaluronic acid solution, alpha-lipoic acid and vitamin E; the weight ratio of the aloe juice, the hyaluronic acid solution, the alpha-lipoic acid to the vitamin E is 200-650 : 100-750 : 0.03-0.1 : 0.5-4; every 100g of the repair liquid contains 40000-4000000 activity unit of SOD; the preparation method is as follows: taking cactus stems and carrying out cell disruption, ultrafilter concentration and multistage precipitation and centrifugal separation process on the cactus stems to obtain crude enzyme supernatant; carrying out three-stage purification process and vacuum drying and grinding on the crude enzyme supernatant to obtain SOD freeze-dried powder; taking aloe plant leaves and carrying out degradation, decoloration, centrifugal separation process and filtration on the aloe plant leaves to obtain the aloe juice; blending the raw materials (components) according to the weight ratio for preparation to obtain the SOD cell repair liquid. The invention has the function of oxidation resistance, can alleviate physical fatigue and strengthen immunity of human body.
CN102670427A Dandruff-removal composition The invention discloses a dandruff-removal composition, which comprises the following components: ketoconazole, clobetasol propionate, vitamin B6, dimethyl sulfoxide, octadecanol, glycerin monostearate, glycerol distearates, cyproheptadine, 2,6-butylated hydroxytoluene and glycerol. Verified by experiments performed by the applicant, the dandruff-removal composition disclosed by the invention is obvious in effect of completely removing dandruffs when being used for dandruff-removal hair care. Moreover, the holding time is long, and dandruffs cannot relapse in at least two years.
US8507477 3- and 6-quinolines with N-attached heterocyclic CGRP receptor antagonists Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.
WO2014044757A1 Cationic triphenylamine derivatives activable by visible and infra red light for inducing and imaging apoptosis in cancer cells The present invention relates to cationic triphenylamines derivatives compounds having a common structure presenting the following general formula (I) activable by visible and infra-red light for inducing and imaging apoptosis in cancer cells (A) where is an optional covalent bond.
WO2012006683A1 Pharmaceutical compositions for sustained delivery of benzodiazepine antagonists The present invention relates to sustained release formulations of benzodiazepine antagonists and their use.
US20080152693 A dopamine agonist and a biodegradable polymer; preferably ropinirole and polylactic acid; side effect reduction; Parkinson's Disease, Attention Deficit Disorder, autism, Asperger's Syndrome, erectile dysfunction, restless leg syndrome, or hyperprolactinemia Biodegradable implants comprising dopamine modulating compounds are described.
CN102228433A Supersaturated self-microemulsion as well as preparation method and application thereof The invention discloses a supersaturated self-microemulsion, comprising Indirubin, an oil phase, a surfactant, a cosurfactant and a supersaturation accelerant. The invention further discloses a preparation method for the supersaturated self-microemulsion and an application of the supersaturated self-microemulsion in the preparation for a medicine treating tumour. The supersaturated self-microemulsion of the invention remarkably increases the bioavailability of Indirubin and has an important significance to enhance the anti-tumour effect of Indirubin.
US20120225941 COMPOSITIONS AND METHODS COMPRISING C16:1n7-PALMITOLEATE One embodiment described herein is related to methods and compositions, such as nutraceutical formulations and dietary supplements, comprising C16:1n7-palmitoleate or derivatives thereof. The methods and compositions comprising C16:1n7-palmitoleate, or derivatives thereof, safely and effectively prevent or mitigate manifestations of cardiovascular disease, including coronary artery disease and the accumulation of cholesterol or lipid deposits in the blood vessels of a subject.
CN1732940A Compound flupentixol and melitracen capsule and preparation process thereof The invention provides an improvement for the dosage form of compound Melitracen and Flupentixol for treating anxiety, depression and asthenia, which is prepared from Melitracen hydrochloride, deflocculating agent and crumbling agent, the weight ratio of Melitracen (C21H25N) and Flupentixol (C23H25F3N20S) is between 40-8:1, the weight ratio of deflocculating agent, crumbling agent and Flupentixol (C23H25FN20S) is between 850-60 : 150-5 : 1.
CN1597671A Quinazoline deriative and preparation method and bioactivity A quinazoline derivative with antineoplastic and plant virus resistant action, its preparing process and its bioactivity are disclosed. An N-aryl substituted 4-aminoquinazoline derivative is prepared from O-aminobenzoic acid or substituent O-aminobenzoic acid through close-loop reaction on formamide, chlorinating, and condensating with arylamine.
US20110236508 L-arginine-based formulation for oral absorption A formulation comprising large quantities of l-arginine and/or fat plaque dissolving agents which is palatable, stench free, and does not evoke nausea. The formulation is adapted to facilitate the adsorption of l-arginine to the blood system and to introduce high levels of l-arginine and/or other fat plaque dissolving agents such as EDTA, its derivatives or its salts into the blood system which are sufficient for effectively dissolving fat plaques in the artery. The formulation comprises at least 10% (w/w) L-arginine, edible organic acids, emulsifier(s), preservatives, flavorings, ethanol and water. Other embodiments may further include chromium salts, and EDTA or its derivatives and their salts
CN1915239A Medication for treating gastric ulcer, duodenal ulcer A medicine for treating gastric ulcer and duodenal ulcer with high curative effect is prepared from chitosan.
US7189743 To inhibit thrombus formation The present invention relates to new compounds of general formula having thrombin-inhibiting activity. Exemplary are: 1-Methyl-2-[4-(N-hydroxyamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-ethoxycarbonylethyl)-amide, and 1-Methyl-2-[4-(N-methoxycarbonylamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-hydroxycarbonylethyl)-amide.
WO2007131286A1 Nanostructures suitable for delivery of agents Novel nanolattices comprising cross-linked or chelated polymers having a desired polydispersity index suitable for delivery of pharmaceutical agents and complexes comprising same are described. Methods of making the nanolattices and use of the nanolattices to deliver pharmaceutical agents for use in a range of diagnostic, prophylactic, therapeutic, nutritional and/or research applications are also described.
US7034041 Substituted 4-phenyl-1-(1-phenylcyclohexyl)-1,2,3,6-tetrahydropyridine Substituted 4-phenyl-1-(1-phenylcyclohexyl)-1,2,3,6-tetrahydropyridine (compounds), methods for the production thereof, pharmaceutical compositions containing said compounds, and methods of treatment of pain and other diseases using the pharmaceutical compositions.
US20110118273 Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
EP2231173A1 Nutraceutical composition and methods of use A method of treatment for cartilage degradation in an organism, which includes administering to an organism a composition including a therapeutic amount of an extract from the plant Biota orientalis. Several key components of the extract of Biota orientalis have been identified that have also been shown to have an effect in dramatically reducing and reversing cartilage degradation.
CN101293888A Xanthine derivative, production and use thereof as a medicament The invention relates to substituted xanthines of general formula (I) wherein R<1> - R<4> are defined as cited in claim 1, the tautomers, stereoisomers, mixtures, prodrugs and salts thereof which exhibit valuable pharmacological properties, particularly an inhibitory effect on the activity of the dipeptidylpeptidase-IV enzyme.
EP1104301B1 Treatment of psychosis or neuropsychiatric symptoms associated with Alzheimer's Disease The use of [R-(Z)]- alpha -(methoxyimino)- alpha -(1-azabicyclo[2.2.2]oct-3-yl) acetonitrile or a pharmaceutically acceptable salt thereof for treatment of psychosis or other neuropsychiatric symptoms in patients with Alzheimer's Disease with severe behavioural disturbance.
CN101838253A Preparation method of ligustilide and butylidene phthalide The invention relates to a method extracting active ingredient from plants, in particular to a method extracting ligustilide and butylidene phthalide from angelica and szechuan lovage rhizome. The method comprises the following steps: raw material smashing, supercritical extraction, solvent extraction, silicagel column separation, high efficiency liquid phase color spectrum preparation, freezing, drying and the like. The content of the finally obtained ligustilide and butylidene phthalide respectively reaches 99.3 percent and 99.5 percent.
US20100239660 Product and use of omega-3s matching human tissue ratios for treatment of inflammatory and other conditions The present invention relates to a product and method for delivering of DHA and EPA in need of omega-3 treatment. It involves administering a liquid formulation such as an oil containing DHA and EPA in a ratio that closely resembles the ratio of DHA and EPA in the human body. The result is a composition that performs as good or better than fish based compositions containing omega-3 fatty acids and can be dosed into smaller volumes when administering mega doses of 1000-2000 mg of DHA to a selected patient.
US20100150944 Methods and compositions for diagnosis and treatment of depression and anxiety The present invention relates to identification of cellular components, genotypes and gene expression profiles associated with mood disorders. In some embodiments, the present invention relates to the correlation between ribosomal protein S6 (RPS6) and depression and/or anxiety. Embodiments of the present invention further relate to regulation of the activity of RPS6, e.g., by p90 Ribosomal S6 protein kinase. Embodiments of the present invention provide methods and compositions for, e.g., diagnosing, treating, and monitoring depression and/or anxiety, or risk thereof, and for selecting, monitoring, and tailoring treatments for depression and/or anxiety.
EP1699444A2 Means for inhibiting viral replication by regulation of protein folding The invention relates to means for treatment of acute and chronic infections with viruses pathogenic to both humans and animals, which assemble at the cell membrane and are released from the cell surface by budding. The above are pathogens for infectious diseases such as AIDS, hepatitis, haemorrhagic fever, SARS, smallpox, measles, polio or flu. Said means contain inhibitors of protein folding as active ingredients, including inhibitors of cellular folding enzymes (enzymatic chaperones) and also substances which block protein folding by chemical chaperones. The following substance classes and derivatives thereof belong to the above: geldanamycin, deoxyspergualin, 4-PBA or herbimycin A. The highly organised processes of the assembly and proteolytic maturation of viral structure proteins are inhibited by said means. As a result the release and production of infectious filial viruses are interrupted.
US20080004344 Novel Salts of Fumaric Acid Monoalkylesters and Their Pharmaceutical Use The present invention relates to novel strontium salts of fumaric acid monoalkylesters. The salts are suitable for use as active substances in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders either alone or in combination with another fumaric acid ester
US20080096965 (Halobenzyloxy) Benzylamino-Propanamides as Sodium and/or Calcium Channel Selective Modulators The invention relates to the use of selected (R)-2-[(halobenzyloxy)benzylamino]-propanamides and the pharmaceutically acceptable salts thereof for the manufacture of medicament, that are selectively active assodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, pain, migraine, periferal diseases, cardiovascular diseases, inflammatory processes affecting all body systems, disorders affecting skin and related tissues, disorders of the respiratory system, disorders of the immune and endocrinological systems, gastrointestinal, urogenital, metabolic and seizure disorders, where the above mechanisms have been described as playing a pathological role.
US20090203731 Treatment of depression and other affective disorders The present invention relates to use of gaboxadol for preparing a pharmaceutical composition for treating depression. Moreover, it relates to the use of gaboxadol for the preparation of a pharmaceutical composition to be used in combination with a serotonin reuptake inhibitor, or any other compound which causes an elevation in the level of extracellular serotonin.
CN101691357B Novel disubstituted imidazolone anti-tumor compounds and preparation method thereof The invention relates to the technical field of medicine, in particular to compounds for inhibiting the growth of tumor cells. A structural general formula of the compounds is as graph, wherein Rs are various substituent groups on the benzene ring, and the substituted positions are not limited and can be 2, 3 and 4. The substitute can be single substitute or multiple substitutes (comprising di-substitute, tri-substitute or tetra-substitute). The compounds specifically comprise (1) H, F, Cl, Br and I; (2) lower alkane such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl and tertiary butyl; (3) lower alkoxy such as methoxy and ethoxy; and (4) hydrogen bond receptor and donor groups such as nitryl, amino and hydroxy. The compounds of the invention have stable chemical properties, can inhibit the growth of the tumor cells, and can be used for preparing anti-tumor medicaments.
CN101267825A Benzodiazepine derivatives for treating hepatitis C infection Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: - R<1> represents C1-6 alkyl, aryl or heteroaryl; - R<2> represents hydrogen or C1-6 alkyl; - each R<3> is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, -CO2R', -CONR'R'', -NH-C0-R', -S(O)R', -S(O)2R', -NH-S(O)2R', -S(O)NR'R'' or -S(O)2NR'R', wherein each R' and R' is the same or different and represents hydrogen or C1-6 alkyl; - n is from 0 to 3; - R<4> represents hydrogen or C1-6 alkyl; - R<5> represents C1-6alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, aryl-C(O)-C(O)-, heteroaryl-C(O)-C(O)-, carbocyclyl-C(O)-C(O)-, heterocyclyl-C(O)-C(O)- or -XR<6>; - X represents -CO-, -S(O)- or -S(O)2-; and - R<6> represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 alkyl)-O-, heteroaryl-(C1-6 alkyl)-O-, carbocyclyl-(C1-6 alkyl)-O-, heterocyclyl-(C1-6 alkyl)-O- or -NR'R'' wherein each R' and R'' is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.
EP1875912A1 Agent for treating involuntary movement The present invention relates to a therapeutic agent for dyskinesia excluding tremor, comprising 1,2-dihydropyridine compound, a salt thereof, or a solvate thereof, which shows AMPA receptor antagonism and is highly useful as a pharmaceutical drug.
US20060287336 S-methyl-dihydro-ziprasidone for treatment of psychiatric and ocular disorders This invention relates to pharmaceutical compositions containing S-methyl-dihydro-ziprasidone and to the use of such compound and its pharmaceutically acceptable salts for the treatment of psychiatric and ocular disorders. More specifically, it relates to the use of such compound and its pharmaceutically acceptable salts for the treatment of a disorder or condition selected from: schizophrenia, anxiety disorders such as generalized anxiety disorder, panic disorder, posttraumatic stress disorder and phobias (e.g., social phobia, agoraphobia etc.); psychotic episodes of anxiety: anxiety, agitation, excessive aggression, tension, or social or emotional withdrawal associated with psychosis; psychotic mood disorders such as severe major depressive disorder; mood disorders associated with psychotic disorders such as acute mania and depression associated with bipolar disorder, and mood disorders associated with schizophrenia; behavioral disturbances associated with mental retardation, autistic disorder, and conduct disorder; dementias such as dementias associated with Alzheimer's disease; drug-induced and neurodegeneration based dyskinesias; obsessive compulsive disorder; Tourette's syndrome; glaucoma; and ischemic retinopathy.
US20090004112 Methods for the treatment of neurodegenerative diseases using nmda receptor glycine site antagonists The disclosure provides methods for treating a neurodegenerative disease by administering a NMDA receptor glycine site antagonist. Compounds that can be used in the methods are also provided. Methods are also provided for determining whether a compound inhibits activity of a Parkinson's Disease-associated mutant of leucine-rich repeat kinase-2 (LRRK2). The methods include assessing accumulation of axonal spheroid inclusions, branching and length of neuronal processes, and neuronal cell death.
CN103340871A Application of Myriberine A in preparation of drug for treating biliary duct cancer The invention discloses application of Myriberine A in preparation of a drug for treating biliary duct cancer, which belongs to the technical field of novel drug use. According to in-vitro MTT (Methyl Thiazolyl Tetrazolium) antitumor activity evaluation, the Myriberine A is found to have a remarkable inhibiting effect for the growth of human biliary duct cancer cell strain RBE (Relative Biological Effectiveness). Therefore, the Myriberine A can be used for preparing the drug for treating biliary duct cancer and is good in development application prospect. The application of the Myriberine A in preparation the drug for treating biliary duct cancer is firstly disclosed; moreover, the inhibitory activity of the Myriberine A to the biliary duct cancer cell is unexpectedly strong.
CN101254173A Soluble semen iris lacteae powder preparations and method of preparing the same The invention discloses a medicament containing irisquinone and a preparation method thereof, and relates particularly to a soluble irisquinone pharmaceutical composition and a formula process for preparing injection thereof, belonging to the technology field of pharmaceutical dosage form and preparations. The preparation method comprises the following steps of dissolving hydroxypropyl-BETA-cyclodextrin in water, and subsequently adding sodium bisulfite; and dissolving irisquinone in anhydrous alcohol, injecting into the above solution, stirring, and freeze-drying or spray-drying to obtain a soluble irisquinone powder preparation, which can dissolve in 0.9% saline water or 5% glucose injection for dilution for oral administration or injection. The technical proposal provided in the invention can effectively increase the solubility and dissolution rate, improve the stability and bioavailability and prolong action time of irisquinone, so as to improve the therapeutic effect and the safety of irisquinone.
US20120141565 Glycerosomes and use thereof in pharmaceutical and cosmetic preparations for topical applications The present invention relates to vesicles for topical delivery of drugs and cosmetics, named glyceromes and characterized by high content of glycerol. The invention further relates to pharmaceutical formulations and cosmetic products containing glycerosomes.
CN103340835A Orally disintegrating tablet suitable for infants and children and preparation method thereof The invention relates to an oseltamivir orally disintegrating tablet which is used for treating the flu of infants and children. The oseltamivir orally disintegrating tablet is prepared from the following ingredients in percentages by weight: 10-40% of taste masking micropill, 20-80% of filling agent, 1-6% of binding agent, 2-10% of disintegrating agent, 0-5% of corrigent and 0.5-2.5% of lubricating agent, wherein the taste masking micropill comprises a medicine containing pill core and a coating layer, the medicine in the medicine containing pill core is oseltamivir or a pharmaceutically acceptable salt of the oseltamivir, which accounts for 10-40% of the total weight of the micropill, the material of the coating layer is polyacrylic resin IV, which accounts for 1-50% of the total weight of the micropill, and the particle size of the micropill is 0.10-0.50mm.
CN101189975A High-grade nutritious calcium replenishing wheaten food The invention relates to the technical field foodstuff manufacturing and aims at solving the problem of providing specific varieties and respective amount of nutriments required by high-grade nutritious cooked wheaten food that has the function of calcium supplement (more particularly bone calcium supplement). The key points of technical proposal of the invention are that: 1. the specific varieties and respective dosage range of the nutriments required by high-grade nutritious cooked wheaten food that has the function of calcium supplement are put forward according to the p of calcium supplement nutriology. 2. the detailed embodiment of various high-grade nutritious cooked wheaten foods that have the function of calcium supplement are provided in light of the concrete situations of various cooked wheaten foods. The invention is designed for Chinese, and has main effects of improving physical health of Chinese people, cancer prevention, ensuring the people to be more vigorous and graceful and osteoporosis and fracture prevention.
EP2033635A1 Short-chain fatty acid derivatives for treating pruritus A method for preventing, treating, or ameliorating pruritus caused by skin, mucosa, or systemic disorder. The method comprises administering to a subject with pruritus or topically applying to an affected area with pruritus an effective amount of a pharmaceutical composition consisting essentially of a phenylbutyric acid or short-chain fatty acid derivative and a pharmaceutically acceptable carrier, salt or solvate thereof.
CN101966194B New application of scutellarin and derivatives thereof The invention provides application of scutellarin and derivatives thereof in the preparation of cranial neuroprotective agents. Taking scutellarin as raw material, structure modification is carried on to obtain apigenin and glycolamide ester of scutellarin, which have obvious cranial neuroprotective activities, and glycolamide ester of scutellarin can permeate the blood-brain barrier to directly reach the target organs, thus being an ideal drug candidate of cranial neuroprotective agents.
EP2598138A2 Aryl hydrocarbon receptor (ahr) modifiers as novel cancer therapeutics Provided herein are novel agents that modulate AhR activity for use in therapeutic compositions and methods thereof for inhibiting cancer cell proliferation and tumor cell invasion and metastasis. The agents comprise AhR inhibitors or non-constitutive AhR agonists of Formula (I) and (II) for the inhibition of cancer cell growth and parameters that characterize tumor metastasis, such as tumor cell invasiveness.
EP1663233B1 Use of tigecycline, alone, or in combination with rifampin to treat osteomyelitis and/or septic arthritis The present invention is directed to a method for treating bone or bone marrow infections, joint infection or infection of the tissues surrounding the joint by administration of the antibiotic tigecycline alone or in combination with a rifamycin antibiotic. In a preferred embodiment the bone or bone marrow infection causes osteomyelitis. In another embodiment the joint infection or infection of the tissues surrounding the joint causes septic arthritis. The invention is also directed to manufacture of a medicament for treatment of bone and/or bone marrow infections, or joint infections and/or infections in tissues surrounding the joint with tigecycline alone or in combination with rifampin.
CN102526371A Medicine for inflammation diminishing, pain stopping, blood activating and detumescence for veterinary use and preparation method thereof The invention discloses a medicine for inflammation diminishing, pain stopping, blood activating and detumescence for veterinary use and a preparation method thereof. The medicine is composed of the following raw material medicines: saffron crocus 1-4g, asarum 2-7g and borneol 7-15g. The preparation method comprises dipping the raw material medicines in 100 milliliter 85% ethanol for 72 hours, filtering and bottling the leach liquor, and preparing the leach liquor into aerosol. The medicine for inflammation diminishing, pain stopping, blood activating and detumescence for the veterinary use and the preparation method of the medicine are convenient, fast, remarkable in curative effect and free of toxic and side effect. In addition, average curative rate of the medicine and the preparation method reaches 91% above.
DE10350929A1 Use of dispirotripiperazine derivatives to treat fungal infections or to prevent adhesion of fungi to surfaces Dispirotripiperazine (3,12-diaza-6,9-diazonia-di spiro(5.2.5.2)hexadecane) derivatives are used to treat fungal infections or to prevent adhesion of fungi to surfaces. - Independent claims are also included for: - (1) pharmaceutical or cosmetic composition comprising dispirotripiperazine derivatives; - (2) washing products, cleaning products, textile treatment products, fabric conditioners, hand washing products, manual dishwashing products, dishwasher detergents and products for treating surfaces, building materials, sealants, filter media, building auxiliaries, ceramics, plastics, metals, textiles, furs, paper, hides, leather or packaging, all containing dispirotripiperazine derivatives; - (3) filter media, adhesives, sealants, packaging, building materials, building auxiliaries, textiles, furs, paper, hides and leather, all containing or treated with dispirotripiperazine derivatives. - ACTIVITY - Fungicide. - MECHANISM OF ACTION - Fungal adhesion inhibitor. 2-Methylmercapto-4-chloro-5-nitrodispirotripiperazine gave 99% inhibition of adhesion of Candida albicans to SK-LMS-1 human leiomyosarcoma cells in vitro at a concentration of 100 micro g/ml.
WO2010113507A1 Double-stranded molecule inhibiting the expression of gpc3 The invention features an isolated double-stranded molecule inhibiting a growth of GPC3 expressing cell. The invention also features a method for treating GPC3-related disease including esophageal cancer, gastric cancer, hepatic cancer, osteosarcoma, soft tissue cancer or endometriosis by administering the double-stranded molecule against a GPC3 gene. Furthermore, the invention features products, including the double-stranded molecules and vectors encoding them, as well as compositions containing the molecules or vectors, useful in the provided methods.
WO2008053861A1 Novel compound having 1,4-benzoxazin-3-one skeleton The object is to synthesize and study a novel compound having a 1,4-benzoxazin-3-one skeleton and find a pharmacological activity of the compound. Specifically provided is a compound represented by the formula [I] or a salt thereof [wherein the ring A represents a benzene ring, a thiophene ring, a thiazole ring, a furan ring or the like; R1 and R2 independently represent a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, an aromatic heterocyclic group or the like; X represents a single bond, C=C, CH2-O, O-CH2, NH-CH2, CH2-NH or the like; Y represents a hydroxyl group, an alkyl group, an alkoxy group, NR3R4 or the like; and R3 and R4 independently represent a hydrogen atom, a hydroxy group, an alkyl group, an alkoxy group, a cycloalkyl group, an aryl group, an aromatic heterocyclic group, a non-aromatic heterocyclic group, or the like.
WO2014021306A1 Medicine against gastroesophageal reflux disease Provided is a medicine to prevent or prevent recurrence of, treat or improve symptoms of gastroesophageal reflux disease for which existing treatments have no effect. 4-[({6-[isobutyl(1,3-thiazole-2-ylsulfonyl)amino]-2,3-dihydro-1H-indene-5-yl}oxy)methyl]-3-methyl benzoic acid, a salt thereof or a prodrug thereof is effective in preventing or preventing recurrence of, treating or improving the symptoms of gastroesophageal reflux disease.
CN102558062A Method for synthesizing imidazole-amino acid derivative and related compound The invention discloses a method for synthesizing an imidazole-amino acid derivative and a related compound, and relates to a method for synthesizing a 2-substituted azole compound shown as a formula (I), the compound shown as the formula (I) and an intermediate compound in the synthesis method.
CN103130848A Macrolide antibacterial compounds, and preparation method and application thereof The invention provides macrolide antibacterial compounds and pharmaceutically acceptable salts thereof. The macrolide antibacterial compounds have a structural general formula represented below, wherein n is 0 or 1, R1 is selected from hydrogen or acetyl, and R is monosaccharide or disaccharide. The invention also provides a preparation method of the compounds and an application thereof in preparing antibacterial medicines. The compounds and the salts thereof provided by the invention are used in preparing antibacterial medicines, and provide advantages such as high efficiency, low toxicity, wide antibacterial spectrum, and the like. Most importantly, with the compounds and the salts, defects such as medicine resistance and poor dissolubility of macrolide antibiotics are solved. Also, the preparation process is simple, and yield is high.
CN1817873A Flavane compound and use thereof A flavane compound and its use are disclosed. In chemical formula, R1 represents H or formula (2), and R2 expresses H or OH. It has anti-inflammatory, anti-allergic and anti-oxidant functions. It can be used for anti-oxidant additive of medicine, food or cosmetics.
US20100292304 Compounds and methods for improving cellular uptake of oligomeric compounds The present invention provides method of optimizing the efficacy and potency of antisense drugs. In certain embodiments, the invention provides assays useful for determining favorable oligonucleotide characteristics and excipeints for improved cellular uptake.
US7074601 Nucleozymes Nucleozymes containing ribonucleotides and deoxyribonucleotides or nucleic acid analogues are described herein. The nucleozymes have catalytic activity and are significantly more resistant to degradation than their all-RNA ribozyme counterparts. Also described are methods for preparing the nucleozymes along with methods of using nucleozymes, e.g., as therapeutic agents.
US20120315345 Functional food and pharmaceutical compositions for anti-obesity comprising capsanthin and fatty-acyl ester of capsanthin having anti-adipogenic activity One or more embodiments of the present invention describe a novel use of capsanthin and/or fatty-acyl ester of capsanthin to inhibit both the differentiation of pre-adipocytes to adipocytes and the accumulation of fat in the adipocytes. One or more embodiments of the present invention are based on findings that capsanthin contained in some natural products such as red pepper, paprika, bell pepper, etc. have anti-adipogenic activity by inhibiting both the differentiation of pre-adipocyte into adipocyte and the accumulation of fat in adipocytes, Therefore, this findings provide a functional food and a pharmaceutical composition wherein capsanthins and the extract of any natural products containing the same components are included in the functional food and the pharmaceutical composition, to offer obesity prevention and/or treatment effects.
CN1615862A Miglitol oral disintegration tablet for treating diabetes II and its preparing method The orally disintegrated miglitol tablet for type-II diabetes consists of main medicine and supplementary material, the main medicine miglitol accounts for 5-50 % and is 10-200 mg in each tablet, and supplementary material consists of stuffing 5-30 wt%, disintegrating agent 5-45 wt%, disintegrating assistant 5-30 wt% and fine silica gel powder 0.1-3 wt% or consists of stuffing 5-30 wt%, disintegrating agent 5-45 wt%, disintegrating assistant 5-30 wt%, adhesive 5-15 wt% and lubricant 0.1-3 wt%. The disintegrated miglitol tablet is prepared with the material powder and through direct or wet tabletting. It is easy to take and can make full use of miglitol in treating diabetes effectively to lower the concentration of blood sugar after meal.
WO2014039839A1 Method of treating leukemia The present invention relates to methods of treating disorders in which DOT1L- mediated protein methylation plays a part, such as cancer, by administering DOT1L inhibitor compounds and pharmaceutical compositions to subjects in need thereof.
CN1814169A Effervescent tablet for treating infant's lung-heat cough and asthma, and preparing method The invention provides an effervescing tablet for curing infantile lung heat and cough and the preparing method thereof, prepared of Ephedra Herb 125g, Bitter Apricot Seed 250g, plaster 1000g, liquorice root 125g, Honeysuckle Flower 417.5g, weeping forsythia 417.5g, Common Anemarrhena Rhizome 417.5g, Baical Skullcap Root 417.5g, Isatis Root 417.5g, Dwarf Lilyturf Tuber 417.5g, Heartleaf Houttuynia Herb 417.5g, lactose, sodium bicarbonate, medicinal citron acid, Asipatan, polyethylene glycol 6000, magnesium stearate; as compared with the existing techniques, it has good taste and flavor and can give out large amounts of CO2 as dissolving in water and is in an effervescing state, thus easy to provoke interests of children and making it not difficult for infants to take, more suitable for children to take, and it is more convenient to carrying and storing.
US7605179 administering vitamin k derivatives for prophylaxis of neurodegenerative diseases associated with protein aggregation or neurofibrillary tangles Provided are napthoquinone-type compounds which can be used to modulate the aggregation of protein (e.g. tau) associated with neurodegenerative disease (e.g. Alzheimer's disease). Structure-function characteristics for oxidised and reduced napthoquinone-type compounds, such as menadione-related compounds, are disclosed. The invention further provides methods of treatment or prophylaxis of neurodegenerative diseases and/or clinical dementias based on the compounds.
EP1147106B1 Process for the preparation of alkyl mercapto methyl ergoline derivatives The present invention relates to the preparation of ingredients active in the treatment of Parkinson's disease, having general formula (VI) wherein R4 may be, independently, a linear, branched or cyclic, saturated or unsaturated C1-8 alkyl radical, such as, for example, the radicals methyl, ethyl, propyl, butyl, isobutyl, tert-butyl, pentyl, cyclopentyl, hexyl, cyclohexyl and octyl. The process for the synthesis of those compounds uses as starting material the compound of formula (I) wherein R1 represents a linear, branched or cyclic, saturated or unsaturated C1-8 alkyl residue.
CN101919875B Preparation method of enteromorpha mushroom polysaccharide compound The invention provides a preparation method of an enteromorpha mushroom polysaccharide compound and application as a health-care medicament thereof. The enteromorpha mushroom polysaccharide compound of the invention consists of enteromorpha polysaccharide and mushroom polysaccharide. By adopting a modern scientific method, the enteromorpha polysaccharide and the mushroom polysaccharide are separated, purified and mixed in a certain ratio to form a polysaccharide compound. The prepared polysaccharide compound has the characteristics of safety, no toxicity, easily obtained raw materials, reliable preparation process and suitability for large-scale industrial production.
US20120077810 Inhibitors Of AKT Activity The instant invention provides for substituted fused pyrimidine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
US20120070519 Method for extraction of fractions containing pharmacologically active ingredients with less cytotoxicity from one or more plants A method of obtaining one or more fractions from one or more plants is disclosed. The method includes subjecting one or more parts of the one or more plants to hydro-alcoholic extraction in presence of a water-insoluble solvent to obtain one or more extracts. The method further includes subjecting the one or more extracts to one or more of de-pigmentation, de-fatting and detoxification process to obtain the one or more fractions. The one or more fractions thus obtained contain a desired pharmacologically active ingredient in concentration greater than concentrations of other pharmacologically active ingredients present in the at least one fraction. Further, the one or more fractions are less toxic as compared with corresponding one or more fractions obtained by conventional methods. In addition, the one or more fractions are therapeutically more effective in various diseases as compared to one or more fractions obtained by conventional methods.
EP2224930A1 Compositions comprising unsaturated fatty acids and nitric oxide releasing compounds and use thereof for enhancing congnitive and related functions Compositions comprising one or more unsaturated fatty acids and one or more nitπc oxide releasing compounds, and methods for using such compositions for enhancing cognitive function, reducing or preventing a decline of social interaction, reducing or preventing age-related behavioral changes, increasing trainabihty, maintaining optimal brain function, facilitating learning and memory, reducing memory loss, retarding brain aging, preventing or treating strokes, and preventing or treating dementia in an animal Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.
CN101081270A Medicine for treating foot helosis, callus and verrucosis The present invention relates to one kind of medicine for treating plantar clavus, callosity and plantar wart. The medicine is prepared with pinellia tuber 480-520 weight portions, safflower 9-15 weight portions, wolfberry bark 18-25 weight portions, and borneol 9-12 weight portions, and through sorting, washing, crushing, sieving, mixing, adding cane sugar in 40-60 weight portions, packing and sealing. It has the advantages of obvious healing effect, no recurrence, simple application and no corrosion.
WO2008086742A1 A medicament for improving the ovum quality and treating female infertility A medicament for improving the ovum quality and treating female infertility, which is composed of vitamin C, nucleotide, zinc gluconate, clomifene, vitamin E acetate, taurine, potassium iodate, and folic acid, and the ratio thereof is from 150: 150: 150: 60: 60: 60: 10: 1 to 70: 70: 70: 40: 40: 40: 10: 1. The preparation method of said medicament comprises the steps of: (1) mixing the components of the medicament in the ratio uniformly, (2) adding excipients and mixing again, (3) drying and formulating into oral preparation. These components of the medicament synergistically reduce toxicity and side effect and improve efficacy.
CN101919860A Medicine composite containing pentoxifyllinum and diclofenac and application thereof The invention relates to a medicine composite containing pentoxifyllinum and diclofenac and application thereof, belonging to the field of medicine. The medicine composite contains two active ingredients, i.e. the pentoxifyllinum and the diclofenac or pharmaceutically acceptable salts thereof, and the proportion of the pentoxifyllinum and the diclofenac or the pharmaceutically acceptable salts thereof is 0.01-10:1 and is 0.1-2:1 preferably. A large quantity of experiment researches show that the medicine composite has outstanding treatment effect on arthritis; and in addition, the experiment researches also prove that the medicine composite also has better improvement action on rat piles models.
WO2008104175A3 Novel phosphodiesterase inhibitors The present invention relates to a compound according to formula I, wherein X, A, G, E, R1, R2, R3 are as shown herein; and pharmaceutically acceptable salts, hydrates, N- oxides or solvates hereof, said compounds are used as phoshodiesterase inhibitors in particular PDE4 inhibitors. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
EP2612860A1 Quinazoline derivatives substituted by aniline, preparation method and use thereof The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.
US20110288055 Mitoquinone derivatives used as mitochondrially targeted antioxidants This invention relates to pharmaceutically acceptable amphiphilic antioxidant compounds, compositions and dosage forms comprising said compounds, and methods and uses reliant on said compounds. The exemplified compounds are all mitoquinone derivatives, being methoxyphenyl alkyl triphenylphosphonium or methoxy dioxocyclohexadiene alkyl triphenylphosphonium derivatives. The compounds, compositions, dosage forms, uses and methods are useful in, for example, the treatment of diseases or conditions associated with oxidative stress.
CN101342160A Application of ocean bromine phenol in preparing medicament for treating antithrombotic forming function The invention relates to a medicine for treating cardiovascular and cerebrovascular diseases, in particular to an application of bromophenol compounds to the preparation of antithrombotic medicine. The bromophenol compounds of the invention have inhibitory activity against thrombin, and can be used for treating various cardiovascular and cerebrovascular diseases caused by thrombotic ischemia.
CN101269023A Natrium pantoprazole sustained-release dropping pill and preparation method thereof The invention discloses a pharmaceutical preparation used for curing active peptic ulcer (gastro-duodenal ulcer), reflux esophagitis and zollinger-ellison syndrome as well as used for curing (1) peptic ulcer hemorrhage, (2) acute gastric mucosal lesion and stress ulcer hemorrhage caused by non-steroid anti-inflammatory drug, and (3) for preventing the weak and narcose patient from having aspiration pneumopleuritis caused by regurgitation and merging of gastric juice after general anesthesia and big surgery, more particularly relates to an oral sustained-release preparation that is prepared by taking methylphenidate hydrochloride as raw material. The invention aims at making up the deficiency of the prior art and provides a methylphenidate hydrochloride sustained-release pill. The methylphenidate hydrochloride sustained-release pill related by the invention effectively overcomes the defects of the prior art and ensures that the medicaments do not have apparent quality change within the valid storing period, at the same time, the methylphenidate hydrochloride sustained-release pill has the advantages of controllable medicine releasing time, enough medicine release and high bioavailability.
CN103263426A New use of gentamicin sulfate as medicament for treating herpes zoster and genital herpes The invention discloses a new use of gentamicin sulfate and specifically relates to the new use as a medicament for treating herpes zoster and genital herpes. An existing gentamicin sulfate injection or a tablet is adopted and matched with an existing analgesic medicament for simultaneous administration, and further used according to an instruction. By using the gentamicin sulfate for treating the herpes zoster and the genital herpes, the advantages of rapid onset of action, short treatment course and low cost can be realized.
CN103059010A 1,4-benzoxazinone-1,2,3-triazole compound having antifungal activity, and its preparation method The invention discloses a 1,4-benzoxazinone-1,2,3-triazole compound having an antifungal activity, and its preparation method. A technical scheme adopted by the invention is mainly characterized in that the structural general formula of the 1,4-benzoxazinone-1,2,3-triazole compound having an antifungal activity is shown in the specification; and in the structural general formula, X can be a halogen atom, an alkoxy group, an alkyl group, NO2, OH, H or CF3, Y is O or S, and R is H, Cl, Br, NO2 or OH. The invention also discloses the preparation method of the compound, and an application of the compound. Eight structures of the 1,4-benzoxazinone-1,2,3-triazole compound have been already synthesized in the invention; the 1,4-benzoxazinone-1,2,3-triazole compound has a certain antifungal activity, and can be well used for controlling the animal and plant diseases caused by fungi; and the preparation method has the advantages of simple and easily-controlled technology, and high yield of the target product.
WO2008114123A1 Spiro benzimidazole derivatives as acid pump inhibitors This invention relates to compounds of the formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, R5, R6, R7, R8 and A are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zollinger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.
CN102558114A Preparation method for vitamin C bulk pharmaceutical The invention relates to a preparation method for a vitamin C bulk pharmaceutical. The method comprises the following steps of: I, stirring vitamin C and sodium carbonate in 70-75 percent ethanol and water for injection till fully dissolving, adding ethylene diamine tetraacetic acid in an amount which is 0.05-0.1 percent of the total feeding weight of the vitamin C, decolorizing with active carbon, filtering a solution, performing aseptic filtration on a filtrate, and pressing into a crystallizing boiler; II, heating the crystallizing boiler in a water bath to 40-50 DEG C, adding absolute ethanol, stirring for 15-30 minutes, cooling the water bath to 5-15 DEG C, and adding vitamin C aseptic powder, wherein the weight ratio of crude vitamin C to the aseptic powder is (5-7):1; and III, filtering a feed liquid, soaking a filter cake which is a crystal with absolute ethanol for 5-10 minutes, leaching, crystalizing, drying in a baking oven, cooling, and sieving a crystal to obtain an aseptic bulk pharmaceutical of the vitamin C. Due to the adoption of the method, the long-term stability, pH value uniformity and content uniformity of a preparation are ensured.
EP1834947A2 3-substituted amino-1H-indole-2-carboxylic acid and 3-substituted amino-benzo[B]thiophene-2carboxylic acid derivatives as interleukin-4 gene expression inhibitors This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Thl/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.
US20100068141 Use of heat shock to treat ocular disease The invention generally provides methods for recruiting stem cells to an ocular tissue. The methods involve inducing heat shock in the ocular tissue using a subthreshold laser and/or an agent. In some embodiments, the heat shock is induced following the administration of an agent that mobilizes HSCs.
US7947835 Certain substituted amides, method of making, and method of use thereof At least one chemical entity chosen from compounds of Formula 2 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
US20100222415 Method to Diagnose, Predict Treatment Response and Develop Treatment for Psychiatric Disorders Using Markers The disclosure provides methods and compositions useful for identifying a subject's predisposition or diagnosis of a mental disorder, methods of screening for agents useful for treating such a disorder and methods of treatment thereof.
WO2013111799A1 Brain function improver The present invention provides a pharmaceutical composition which contains a compound represented by formula (I) and can be used for the improvement of the brain function.
CN101601683A Medicinal composition for reducing blood sugar and blood lipid and treating diabetes The invention discloses a medicinal composition for reducing blood sugar and blood lipid and treating diabetes, which comprises berberine, radix astragali, vitamin A, beta-carotene, vitamin B complex, vitamin C, vitamin D, vitamin E, macroelements, namely calcium, potassium and magnesium, and microelements, namely zinc, selenium, iron, chromium, copper, molybdenum, iodine and manganese. The medicinal composition is mainly suitable for the crowds with hyperglycemia, hyperlipidemia and the diabetes, has obvious effect in the aspects of reducing the blood sugar and the blood lipid and treating the diabetes, and can be applied for long time or applied according to course of treatment.
US20070105918 Use of Pramipexole to Treat Amyotrophic Lateral Sclerosis The present invention is directed to compositions comprising pramipexole and the use of such compositions to treat neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS). As shown in FIG. 6B the mean +/− SEM serum 2.3 DHBA levels for the 12 ALS participants decreased significantly after pramipexole treatment.
US7723496 Tumor antigen for diagnosis and treatment of cell proliferative disorders A compound inhibiting the activity of a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 4, SEQ ID NO: 7, SEQ ID NO: 10, SEQ ID NO: 15, SEQ ID NO: 17, SEQ ID NO: 20, SEQ ID NO: 22, SEQ ID NO: 25 or SEQ ID NO: 27, or a salt thereof; a compound inhibiting the expression of a gene of the protein; an antisense polynucleotide containing the entire or part of a base sequence complementary or substantially complementary to a base sequence of a polynucleotide encoding the protein or its partial peptide; an antibody to the protein or its partial peptide, etc. are useful as prophylactic/therapeutic agents for cancer, etc., apoptosis promoters for cancer cells, and the like.
US20110129515 Devices and Methods for Nerve Regeneration The present invention is directed to a nerve regeneration conduit including a resorbable tube having a matrix therein. The matrix is characterized by substantially parallel, axially aligned pores extending the length of the matrix. The matrix is formed by the axial freezing of a slurry having little or no significant radial thermal gradient during the freezing process. The matrix is used to bridge the gap between the severed ends of a nerve and provide a scaffold for nerve regeneration.
CN101259118A Application of 2',4'-dihydroxy-6'-methoxy-3',5'-dimethyl chalcone as PPAR gamma agonist The invention discloses an application of 2',4'-dihydroxyl-6'-methoxyl-3',5'-dimethyl chalcone as an agonist of PPAR-gamma of a peroxisome growth factor; the application of the compound as the agonist of the PPAR-gamma provides a novel drug for preventing and treating type II diabetes, hyperlipemia and adiposity.
EP1708996A1 Fused heteroyral derivatives for use as p38 kinase inhibitors Compounds of formula (I) are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
EP1401425B1 Organometallic anti-tumour agent The invention relates to complexes of general formula D2-M-T, wherein D represents a beta -diketone, M represents a metal atom and T represents a substance comprising at least one group containing N, O or S. The invention also relates to the use of said complexes as anti-tumour agents.
US20110003783 Nicotinic acid compositions for treating hyperlipidemia and related methods therefor An orally administered antihyperlipidemia composition according to the present invention includes from about 250 to about 3000 parts by weight of nicotinic acid, and from about 5 to about 50 parts by weight of hydroxypropyl methylcellulose. Also, a method of treating hyperlipidemia in a hyper lipidemic having a substantially periodic physiological loss of consciousness, includes the steps of forming a composition having an effective antihyperlipidemic amount of nicotinic acid and a time release sustaining amount of a swelling agent. The method also includes the step of orally administering the composition to the hyperlipidemic once per day “nocturnally,” that is in the evening or at night,
US20080261942 Combinations of bile acid sequestrant(s) and sterol absorption inhibitor(s) and treatments for vascular indications The present invention provides compositions, therapeutic combinations and methods including: (a) at least one bile acid sequestrant; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.
WO2008071421A1 Nitrate esters of carbonic anhydrase inhibitors Nitroderivatives of carbonic anhydrase inhibitors having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma, ocular hypertension, age-related macular degeneration, diabetic macular edema, diabetic retinopathy, hypertensive retinopathy and retinal vasculopathies, cancer, epilepsy, high-altitude disorders and neuromuscular diseases.
EP1809381A2 Use of compounds for the prevention of drug-induced cell toxicity The present invention relates to the use of compounds for the manufacture of a medicament for the prophylaxis and/or treatment of induced cell toxicity, such as nephewrotoxicity and ototoxicity, in particular where the cell toxicity is induced by a medical treatment. In a preferred embodiment, the compounds have at least two nitrogen atoms, more preferably at least two amino groups. The compounds according to the invention are capable of docking binding of cell toxic compounds to the megalin receptor, and thereby inhibiting uptake of the cell toxic compounds into cells. The invention further relates to novel compounds for use in said treatment, as well as a method for reducing the cell toxicity of cell toxic compounds.
CN103705510A Method for preparing azilsartan solid composition The invention discloses a method for preparing an azilsartan solid composition. The preparation method comprises the following steps: (1) adding water into azilsartan API (not subjected to micronization) and an adhesive for uniformly mixing to obtain a suspension solution I; (2) performing wet grinding on the suspension solution I to obtain a suspension solution II; (3) adding the suspension solution II into a diluent of a pharmaceutical composition in an injection mode, and drying to prepare granules and powder of an azilsartan pharmaceutical composition; (4) preparing the granules and powder into the medical minimum dose unit of azilsartan. The method has the beneficial effects that the problem that related substances are rapidly increased in the process of preparing azilsartan particles by adopting a conventional grinding method is solved, and the storage period of the azilsartan preparation is favorably prolonged.
CA2260943C Formulation of 5-ht agonists This invention comprises a method of treating migraine in a human comprising co-timely administering of a therapeutically effective amount of a 5-HT agonist coordinated with a therapeutically effective amount of an analgesic, particularly a long-acting NSAID, and in some instances, doses below those ordinarily considered as minimum effective doses as to one or both 5-HT agonist and long-acting NSAID. Dosage forms are also included herein.
EP2069333A1 Pyrrole derivatives useful for the treatment of cytokine-mediated diseases A compound of Formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the groups R1-R6 and A are as defined in the specification.
CN103099807A Compound zinc gluconate and ibuprofen oral-administration composition for covering bitter taste and improving ibuprofen dissolution The invention relates to the field of pharmaceutic preparation, and specifically relates to a compound zinc gluconate and ibuprofen oral-administration composition for covering bitter taste and improving ibuprofen dissolution check item, and a preparation method thereof. The compound zinc gluconate and ibuprofen oral-administration composition for covering bitter taste and improving ibuprofen dissolution is characterized by mainly comprising main drugs: 0.036-0.83 of high-sweetness sugar, 5-15 of filler, and 0.0006-0.0060 of surfactant. The preparation provided by the invention is good in taste and high in bioavailability; and the composition is blended with water before administration so that the compliance of patients is improved.
CN101002795A Method for preparing dialysis dry powder and dialysate of pure sodium bicarbonate A dried powder or liquid of medical high-purity sodium dicarbonate for dialysis with portable artificial kidney (blood dialysis machine) MR-100 to treat renal failure, uremia, poisoning and gout is prepared from sodium chloride and high-purity sodium dicarbonate. Its preparing process is also disclosed.
EP1725565A2 Fused heterotricyclic compounds as inhibitors of 17b-hydroxysteroid dehydrogenase 3 Fused heterotricyclic compounds, methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer, and pharmaceutical compositions containing such compounds.
CN101507739A Biological agent containing human ARMET protein or oligonucleotide active constituent and use thereof The invention relates to a biological preparation taking human ARMET protein or oligonucleotide as an active ingredient. The biological preparation is characterized in that the biological preparation at least contains the human ARMET protein or interfering oligonucleotide of the human ARMET protein (siRNA or miRNA) which is taken as the active ingredient of the biological preparation. Other active ingredients or pharmaceutically acceptable excipients can also be added. The biological preparation has good solubility and stability and easy preparation, and shows remarkable neuroprotection, anti-antarthritic effect and antitumor effect.
US20100068262 Method and Compositions for Stimulation of an Immune Response to PSMA using a Xenogeneic PSMA Antigen Tolerance of the immune system for endogenous PSMA can be overcome and an immune response stimulated by administration of xenogeneic or xenoexpressed PSMA antigen. For example, mouse PSMA, or antigenically-effective portions thereof, can be used to stimulate an immune response to the corresponding differentiation antigen in a human subject. Administration of xenogeneic antigens in accordance with the invention results in an effective immunity against PSMA expressed by the cancer in the treated individual, thus providing a therapeutic approach to the treatment of cancers expressing PSMA, such as prostate cancer.
CN101318943A Substituted diethylenediamine compounds, preparation method, uses and medicament composition containing the compounds The invention relates to substituted piperazines compounds shown in formula (I), a preparation method, an application thereof, and a drug composition containing the compounds. The compounds shown in the formula (I) can be antagonists and/or inverse agonists of cannabinoide-1 receptor (CB1), can be used for treating, preventing and inhibiting diseases mediated by the CB1 receptor, and can be used for preparing medicines for treating obesity, mental diseases and nerve diseases.
US20110150778 Assembly of Gas-Filled Microvesicle With Active Component For Contrast Imaging Assembly comprising a gas-filled microvesicle and a structural entity which is capable to associate through an electrostatic interaction to the outer surface of said microvesicle (microvesicle associated component—MAC), thereby modifying the physico-chemical properties thereof. Said MAC comprises a targeting ligand a diagnostic agent or any combination thereof. Optionally a bioactive agent can further be associated to the MAC. The assembly of the invention can be formed from gas-filled microbubbles or microballoons and a MAC having preferably nanometric dimensions, e.g. a micelle, and is used as an active component in diagnostically and/or therapeutically active formulations, in particular for enhancing the imaging in the field of ultrasound contrast imaging, including targeted ultrasound imaging, ultrasound-mediated drug delivery and other imaging techniques such as molecular resonance imaging (MRI) or nuclear imaging.
US20100063103 (3-{[2-(Benzenesulfonyl)pyridin-3-yl]methyl}-5-fluoro-2-methylindol-1-yl)-acetic acid, used in the treatment of allergic or inflammatory diseases mediated by prostaglandin D2 (PGD2) or other agonists acting at the oattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) receptor Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
CN1989953A Composition of ambroxol, salt thereof and anti-infective drug The invention belongs to the field of medical technology, and discloses a medicinal combination which contains ambroxol or its pharmaceutical acceptable salt and at least one anti-infective drug and their preparation methods and uses. Among them, the anti-infective drugs selected from: baicalin and/or 14-dehydroxylation-11, 12-two-dehydrogenating-andrographolide-3, 19-two succinic acid half ester salt, the drug combinations can be made to various pharmaceutical acceptable formulations; combinations are used to preparing and treating upper respiratory tract infection, chronic bronchitis, pneumonia and exfoliative viscous, expectoration difficulty and other disease leading by upper respiratory tract infection(such as acute, chronic bronchitis, bronchial asthma, bronchiectasis and phthisis confirmata and so on), and has synergic synergism and the stability is fine, its effect is improved greatly compared to only using same dosage alcaine ambroxol or baicalin or Yanhuning, it produces unexpected results and has extensive application prospects.
CN101665473B Substituted benzene propenyl piperazinyl alkyl polyhydric benzamide compound and preparation method and application thereof The invention relates to a (E)-N-3-(4-substituted benzene propenyl piperazine-1-base) alkyl benzamide compound shown in a formula (I) or a salt thereof, wherein R<1>, R<2> and R<3> express -H, -OH, -ONa, -OK or -ONH4, R<4> and R<5> express-H, halogen, C(1-3) linear or branched alkyl, -OH, -ONa, -OK, -ONH4, -NO2 or -CN, and n is an integer of 1-3. The invention also relates to a preparation methodof the compound, which comprises the following steps: synthesizing multi-alkoxy benzoyl chloride substituted alkylamine by using multi-substituted benzoyl chloride and hydrochloride of chlorinated alkyl amino as raw materials; carrying out reaction on the compound and piperazine to prepare N-piperazinyl alkyl multi-substituted benzamide; reacting with substituted benzene acryloyl chloride to prepare (E)-N-3-(4-substituted benzene propenyl piperazine-1-base) alkyl benzamide; acting with BBr3 or BF3 aether solution to be further hydrolyzed to generate the corresponding (E)-N-3-(4-substituted benzene propenyl piperazine-1-base) alkyl polyhydric benzamide compound, and then reacting with alkaline to generate the corresponding salt. The compound has inhibition function to HIV-1 integrase.
WO2009023471A2 Compositions comprising a dissociated glucocorticoid receptor agonist for treating or controlling anterior-segment inflammation A composition for treating or controlling an inflammatory anterior-segment disease or condition comprises a dissociated glucocorticoid receptor agonist ('DIGRA'). The composition can optionally include an anti-inflammatory agent, an anti-infective agent, or both. The composition can be formulated for topical application, injection, or implantation in the anterior portion of the eye or a tissue adjacent thereto.
US20120083518 Cancer Treatment Targeting BRCA1-IRIS Patients identified as candidates at risk of developing aggressive cancer, including metastatic cancer, are determined based on the expression of BRCA1-IRIS. In one advantageous form, the expression of BRCA1-IRIS is quantified based on BRCA1-IRIS present in tumor cells of patients. The amount of BRCA1-IRIS expression can be quantified in any conventionally known manner, including quantifying the amount of protein present in tumor cells or BRCA1-IRIS mRNA present in tumor cells of patients.
CN101583715A Inhibitory polynucleotide compositions and methods for treating cancer Compositions and methods for treating diseases, such as cancers. The compositions are effective to silence, down-regulate or suppress the expression of a validated target gene by stimulating the process of RNA interference of gene expression, thus inhibiting tumor growth. The invention also provides methods for treating diseases, such as cancers, by inactivation of a validated target gene product, using neutralizing antibody or small molecule drug, to inhibit tumor growth. More particularly, the compositions and methods are directed toward a cancer or a precancerous growth in a mammal, associated with pathological expression of a certain target genes identified herein. The compositions inhibit expression of the target gene when introduced into a tissue of the mammal. The methods include administering the compositions of the invention to a subject in need thereof in an amount effective to inhibit expression of a target gene in a cancerous tissue or organ.
US20130029949 Substituted Quinolines and Their Use As Medicaments Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.
CN103611049A Preparation method of composition for treating rumen indigestion of beef cattle The invention provides a preparation method of a composition for treating rumen indigestion of beef cattle, which comprises the following steps: A. preparing Fructus Forsythiae, phellodendron bark, rhubarb, hawthorn, picrorhiza rhizome, mirabilite, alcoholic rhizoma anemarrhenae, alcoholic golden cypress, medicated leaven, moleplant seed, fructus aurantii, dried orange peel, bush-cherry seed, honied radix astragali, dangshen, amomum fruit, pawpaw, tuckahoe, agilawood, Chinese yam, figwort and licorice; B. immersing the active pharmaceutical ingredients in water for 30 minutes to 1 hour, heating for boiling for 30 minutes, and filtering to obtain the filtrate for later use; adding water into the filter residue, heating for the second time, boiling for 30 minutes, and filtering to obtain the filtrate for later use; adding water into the filter residue, heating for the third time for boiling for 40 minutes, and filtering; and merging the three filtrates, heating to concentrate to a paste, putting in a drying oven, drying while controlling the temperature at 80 DEG C, cooling, mixing with honey, kneading into strips, making pills, sealing with wax and packaging. The composition is simple in proportioning and convenient to use, and is used for clearing away heat and toxic material, activating blood circulation to dissipate blood stasis, promoting circulation of qi and to relieve pain, strengthening the spleen, stimulating the appetite, strengthening the middle-jiao, invigorating qi, removing heat from the blood and promoting salivation.
CA2839790A1 Rapid dissolve tablet compositions for vaginal administration Disclosed herein are pharmaceutically acceptable rapid dissolve vaginal tablet compositions comprising one or more active pharmaceutical ingredients suitable for therapy via topical action or systemic absorption, and methods of making and using such compositions. In some embodiments, this invention relates to pharmaceutical compositions comprising one or more active pharmaceutical ingredients suitable for vaginal route of administration, and methods of making and using such compositions for therapy via topical action or systemic absorption, as well as uterine targeting. In certain embodiments, the present invention is related to a pharmaceutical composition comprising one or more active pharmaceutical ingredients suitable for vaginal route of administration, one or more polymeric excipients having a dual property of acting as a binder as well as a bioadhesive material, one or more sugar alcohols or saccharides, and one or more disintegrants.
CN103330942A Florfenicol smell masking preparation and preparation method thereof The invention discloses a florfenicol smell masking preparation and a preparation method thereof and belongs to the field of antibiotic preparations for livestock. The florfenicol smell masking preparation is prepared through melt extrusion by taking florfenicol, stomach soluble polyacrylic resin, talcum powder and glycerin monostearate as raw materials. Compared with the prior art, the florfenicol smell masking preparation has the characteristics of good dissolution and smell masking effects, is convenient for continuous mass production and has good popularization and application values.
EP2204178A1 Laxative agent A laxative agent comprising composite magnesium oxide particles represented by the following formula (1) as an effective component: M g 2 + 1 − x Z n 2 + x O x i s 0.0001 t o 0.3. . The laxative agent is excellent in the effect of protecting the mucosa of a digestive organ.
EP2526940A2 Compositions containing enantiomeric equol, and methods for their making A composition for use in making commercial food and skin products, comprising S-equol, or R-equol, or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.
US7015237 Pyridine matrix metalloproteinase inhibitors Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.
WO2010056877A2 Haloalkyl containing compounds as cysteine protease inhibitors The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
US20120053195 Hydrobromide salts of a pyrazolylaminoquinazoline Provided herein are hydrobromide salts of a pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating a proliferative disease.
CN101959525A Anti-methicillin-resistant staphylococcus aureus agent and anti-vancomycin-resistant enterococcus agent Disclosed are an anti-methicillin-resistant Staphylococcus aureus agent (an anti-MRSA agent) and an anti-vancomycin-resistant Enterococcus agent (an anti-VRE agent), each of which comprises, as an active ingredient, an Macaranga tanarius extract that is extracted from a plant Macaranga tanarius with an extraction solvent comprising at least an organic solvent. Alternatively, each of the anti-MRSA agent and the anti-VRE agent may comprise at least one member selected from nymphaeol-A, nymphaeol-B and nymphaeol-C as an active ingredient.
WO2009004329A1 9h-pyrimido[4,5-b]indoles, 9h-pyrido[4',3':4,5]pyrrolo[2,3-d]pyridines, and 9h-1,3,6,9-tetraaza-fluorenes as chk1 kinase function inhibitors The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4',3':4,5]pyrrolo[2,3-d)pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or Il inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.
WO2011118682A1 Aptamer for ngf and use thereof Disclosed is a better quality aptamer having binding activity on NGF. This aptamer binds to NGF satisfying (1) and (1): (1) Includes a sequence expressed by UGAAARAAACC (SEQ ID NO: 64) or CGAAMRAAACU (EQ ID NO: 65). (2) Length of 73 bases or less.
WO2005007651A1 2-acylaminothiazole derivative or salt thereof It is intended to provide a 2-acylaminothiazole derivative which has an activity of increasing platelets based on excellent effects of proliferating human c-mpl-Ba/F3 cells and promoting megakaryoblast colony formation and is useful in treating thrombopenia.
WO2008014686A1 Formulation containing low molecular heparin for intraarticular injection A formulation containing low molecular heparin for intraarticular injection, which can evidently ameliorate and treat rheumatic arthritis, rheumatoid arthritis, osteoarthritis, synovitis and/or cartilage injure.
US20120029045 Method for treating port wine stains A method of using photodynamic therapy to perform selective targeted therapy of biological tissue. The method includes intravenously injecting a porphyrin-based photosensitizing drug followed by irradiating the tissue with light while the drug is being injected. The duration of the irradiation and other parameters are controlled so that the selected biological tissue is treated and non-selected tissue is not damaged. By controlling the flow rate of the injection and other parameters, so that irradiation of the effected tissue overlaps with injection of drug, the target tissue is effectively treated without damage to non-target tissue.
CN102579532A Radix acanthopanacis senticosl composition, preparation containing composition and detection method of preparation The invention relates to a radix acanthopanacis senticosl composition, a preparation containing the composition and a content detection method of the preparation. The composition per gram contains 50-120mg of total flavones, 12.5-30mg of syringin and 4-15mg of eleutheroside E. The composition and preparation provided by the invention have effects on lowering blood sugar level, lowering blood lipid and treating male sterility and have better effects than the prior art.
US20050038248 Chemotherapeutic agents The invention provides 1,2-substituted cyclic compounds useful for treatment of diseases or disorders arising from abnormal or inappropriate cell proliferation, such as tumour growth, tumour metastasis and associated angiogenesis, as well as pharmaceutical compositions comprising these compounds and their use in methods of treatment.
WO2014105635A1 Sterile ophthalmic pharmaceutical suspensions An aqueous suspension of a carbonic anhydrase inhibitor such as brinzolamide as well as methods of preparation thereof, are disclosed. The suspension comprises an organic polar solvent such as dimethyl sulfoxide and/or a non-aromatic non-ionic polyethoxylated surfactant such as polyethoxylated castor oil and/or or polysorbate 80. Methods include precipitating brinzolamide from the heated composition. Methods also include sonication of the suspension to reduce brinzolamide particle size.
WO2013187965A1 Pyrazole derivatives as inhibitors of stat3 Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.
US20080076755 4-(Adamantane-1-carbonylamino)-3-oxo-2-aza-bicyclo[2.2.2]octane; 5-(Adamantane-1-carbonylamino)-10-oxo-9-aza-bicyclo[3.3.2]decane for treating autoimmune diseases, vascular disorders, viral infection or replication, asthma, osteoporosis, tumor growth, rheumatoid arthritis, organ transplant rejection The invention provides compounds, compositions, and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, for the preparation of a medicament intended to treat an inflammatory disorder wherein y is any integer from 1 to 8; z is any integer from 1 to 8; with the proviso that y and z cannot both equal 1; X is —C —(Y)k—(R1)n or SO2—(Y)k (R1)n; k is 0 or 1; Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or Y is a cycloalkenyl or polycycloalkenyl group.
CN201996872U Oral-administration active carbon alcoholism-relieving capsule The utility model relates to an oral-administration active carbon alcoholism-relieving capsule comprising a capsule shell and a contained material which is contained in the capsule shell and comprises active carbon particles. The oral-administration active carbon alcoholism-relieving capsule is simple in structure and small and exquisite in size. With powder made from active carbon and auxiliary material being put in the capsule shell, the capsule is available to be carried around. The capsule is administrated for relieving alcoholism with a good and quick drug effect. Meanwhile, the oral taste of the capsule is improved.
CN101961491A Novel blood pressure and blood fat reduction composition The invention discloses a novel blood pressure and blood fat reduction composition. The composition is prepared by compounding amlodipine and magnesium statins which serve as active ingredients, and pharmaceutically acceptable auxiliary materials, wherein the amlodipine further comprises medicinal salts, optical isomers and hydrates thereof; and the magnesium statins are magnesium salts of statin compounds. The composition can be prepared into an oral preparation and is used for the long-term treatment of hypertension and hyperlipidemia.
US20100204195 Pharmaceutical Compositions and Process for Making Them Amorphous HMG CoA reductase inhibitors, especially amorphous atorvastatin, are described. Also described are pharmaceutical combinations comprising amorphous HMG CoA reductase inhibitors in combination with cholesterol absorption inhibitors or fibrates. A method of manufacturing the compositions using a hot melt extrusion process are also described.
WO2007145239A1 Anti-fatigue agent containing amino acid composition It is intended to provide an anti-fatigue agent capable of preventing both muscle fatigue and nerve fatigue simultaneously. According to the invention, both muscle fatigue and nerve fatigue can be simultaneously prevented with the anti-fatigue agent containing an amino acid composition comprising specific types and specific amounts of amino acids. With regard to preferred amino acid types and amount ratios, it is an amino acid composition containing 30 to 200 parts by weight of proline, 60 to 140 parts by weight of glycine, 25 to 260 parts by weight of alanine, 40 to 130 parts by weight of lysine, 20 to 75 parts by weight of tryptophan, and 15 to 40 parts by weight of histidine. Further, it preferably contains 35 to 65 parts by weight of threonine, 15 to 65 parts by weight of tyrosine, and 25 to 45 parts by weight of arginine, and further, it preferably contains 30 to 55 parts by weight of valine, 35 to 60 parts by weight of leucine, and 25 to 45 parts by weight of isoleucine.
US20100112063 Method for preparing a hydrogel adhesive having extended gelation time and decreased degradation time A method for extending the gelation time of an oxidized polysaccharide to react with a water-dispersible, multi-arm amine to form a hydrogel is disclosed. The extension of the gelation time is accomplished by using a chemical additive. The method also extends the time for the hydrogel to become tack-free, and may also be used to decrease the degradation time of the hydrogel. The chemical additive reacts with the functional groups of the oxidized polysaccharide or the water-dispersible, multi-arm amine, thereby reducing the number of groups available for crosslinking. The use of the resulting hydrogel for medical and veterinary applications is described.
US20100204244 Agents for treatment of diabetic retinopathy and drusen formation in macular degeneration Agents that stimulate nuclear translocation of Nrf2 protein and the subsequent increases in gene products that detoxify and eliminate cytotoxic metabolites are provided in a method for treating diabetic retinopathy or drusen formation in age-related macular degeneration. The structurally diverse agents that act on the Nrf2/ARE pathway induce the expression of enzymes and proteins that possess chemically versatile cytoprotective properties and are a defense against toxic metabolites and xenobiotics. Agents include certain electrophiles and oxidants such as a Michael Addition acceptor, diphenol, thiocarbamate, quinone, 1,2-dithiole-3-thione, butylated hydroxyanisole, flavonoid other than genistein, an isothiocyanate, 3,5-di-tert-butyl-4-hydroxytoluene, ethoxyquin, a coumarin, combinations thereof, or a pharmacologically active derivative or analog thereof.
WO2009147169A1 Pharmaceuticl compositions useful for the treatment of cancers, in particular acute myeloid leukemia and acute promyelocytic leukemia The present invention relates to new pharmaceutical compositions useful for the treatment of cancers, in particular acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL). The compositions comprise retinoic acid or a related compound in combination with at least one phosphodiesterase inhibitor or at least one agent enabling to increase the cellular content of cAMP. The compositions may further comprise an arsenic derivative.
US8618086 Compositions and methods for treating hair loss using C16-C20 aromatic tetrahydro prostaglandins A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
WO2014098190A1 Composition and food or drink A composition which comprises γ-oryzanol and biocompatible particles containing γ-oryzanol enclosed therein. The biocompatible particles may comprise a polylactide glycolide copolymer, which is optionally modified with polyethylene glycol, having a number-average particle size of 2.5-1,000 nm. The aforesaid composition is to be used for improving insulin resistance. Also, the composition is to be used for treating or preventing a disease selected from the group consisting of obesity, dyslipidemia, impaired glucose tolerance, diabetes, arteriosclerosis and inflammatory diseases.
CN101606913A Cefixime dispersing tablet and preparation methods thereof The invention discloses a cefixime dispersing tablet and preparation methods thereof, belonging to the technical field of pharmaceutical preparation. The cefixime dispersing tablet comprises 40-420 mg of cefixime, 0-100 mg of starch, 0-250 mg of amylum pregelatinisatum, 10-80 mg of mannite, 0-150 mg of microcrystalline cellulose, 10-60 mg of carboxyrnethyl starch sodium, 2-20 mg of polyvidone K30, 0.4-10 mg of magnesium stearate, 0-10 mg of Steviosin and 0-10 mg of orange compound perfume. The preparation method comprises the following steps: evenly mixing basic remedies and excipients; adding adhesive to prepare granulates; drying; sorting and then adding with other excipients; and tabletting. The other preparation method is described as follows: the basic remedies are added after granulating. The invention aims to solve the technical problem that cefixime preparation has shorter disintegration time, better leachability, higher content of the basic remedies, production cost reduction, quality detection time reduction and production environment pollution reduction.
US7094802 PKB-3564 substance with neovascularization inhibitory activity A compound represented by formula (I) wherein R1 represents hydrogen atom and R2 represents hydroxyl group, or R1 and R2 may combine together to represent oxo group or oxime group; R3 represents hydrogen atom and R4 represents hydroxyl group, or R3 and R4 may combine together to represent oxo group or oxime group; R5 represents hydrogen atom and R6 represents hydroxyl group, or R5 and R6 may combine together to represent oxo group or oxime group; R7 represents hydrogen atom and R8 represents hydrogen atom, or R7 and R8 may combine together to represent oxo group or oxime group; R9 and R10 represent hydrogen atom, an alkyl group, or an alkenyl group. The compound is useful as an active ingredient of a medicament having angiogenesis suppressive activity, apoptosis suppressive activity, and cell cycle inhibitory activity
CA2261972C Method of breeding high-level lactation dairy cows using rumen-bypassed amino acids Lysine and methionine which are limiting amino acids of dairy cows are administered to dairy cows to decrease the BUN value that has an adverse effect on the conception rate and to increase the blood glucose required to improve the energy balance, that alanine and glutamine are administered to dairy cows to increase the blood glucose and to improve the liver function, and that the use of these amino acids is effective for keeping good conditions of dairy cows, allowing earlier arrival of initial estrus without any stress, improving the mating conception rate and decreasing the non-conception rate.
CN103330119A Health-care food for accessorily reducing blood fat The invention discloses a health-care food for accessorily reducing blood fat, and the health-care food is prepared from the following raw materials in parts by weight: 30-40 parts of chitosan, 5-15 parts of hawthorn extractives, 10-20 parts of ginkgo leaf extractives, 15-25 parts of cassia seed extractives, 10-25 parts of radix notoginseng extractives and 7-20 parts of grape seed extractives. The health-care food for accessorily reducing the blood fat, which is disclosed by the invention, obviously reduces the blood fat and the cholesterol, enhances the action of high density lipoprotein, well achieves the health-care functions of accessorily reducing the blood fat, blood pressure and blood sugar and is an ideal health-care food for middle-aged and elderly hypertension, hyperlipemia and hyperglycemia people.
US20120195988 Therapeutic Uses for Plants of the Capsicum Genus A saponin or a sapogenin, or a saponin or sapogenin derivative, from a plant of the capsicum genus for use in the treatment of a disease other than eczema and dermatitis. A process for preparing a plant of the capsicum genus, extracts, or seeds thereof for use as a medicament suitable for the treatment of diseases other than skin conditions which process comprises storing the plant, extracts or seeds thereof at a temperature of 20° C. or below.
US20060252732 Blood vessel-growth promoter A neo-vascularization promoter containing acetylsalicylic acid or its pharmaceutically acceptable salt as an active ingredient.
US20080025951 Administering to an individual having acute liver disease or inflammatory skin disease a carrier and a specific polypeptide that contains signal peptide sequences and a transmembrane spanning domain This invention relates to novel uses of a protein sequence (INSP052EC), herein identified as an immunoglobulin domain-containing cell surface recognition, in the diagnosis, prevention and treatment of diseases, in particular those related to the excessive expression and/or secretion of cytokines.
US20080221120 Identify pyrazole imine derivatives that modulate activity of aquaporin-; culturing a cell expressing an aquaporin-1 (AQP1) in the presence of an agent, determine effect on cell migration, cell adhesion, cell proliferation; treat cellular proliferative disease, cancer The invention provides compositions, pharmaceutical preparations, and methods for modulating angiogenesis and/or cell migration in a subject having a cellular proliferative disease (e.g., cancer), or a disease or condition amenable to treatment by enhancing cellular proliferation and cell migration (e.g., angiogenesis), by modulating the activity of an aquaporin, such as aquaporin-1. The compositions and pharmaceutical preparations of the invention may comprise one or more of compounds that modulate the activity of aquaporin-1.
CN1785007A Method for preparing soymilk powder contg. micron ginseng, antler, pearl and pollen pini for tonifying-Yang, dispelling-fatigue and enriching-calcium A micron-class health-care bean milk powder for invigorating Yang, relieving fatigue and supplementing Ca is prepared from traditional bean milk powder, micron-particles of ginseng, antler, pine pollen and pear, and oligose through proportional mixing, processing and fermenting. Its advantages are high effect and rich nutrients including vitamins, minerals, etc.
EP1255535B1 Controlled release pharmaceutical composition containing tramadol hydrochloride The invention solves a controlled release pharmaceutical composition containing tramadol hydrochloride, characterized in that it contains 100 to 200 mg of the active ingredient in admixture with micronized esters of glycerol with higher fatty acids, alkali salts of phosphoric acid, non-ionic vinylpyrrolidone polymers, substances from the group of salts of higher fatty acids with alkaline earth metals and silicon oxides and a method for the preparation of this composition.
CN101456845B 4,5-diaryl-2-sulfhydryl miazines compounds and synthetic method thereof and pharmaceutical use The invention provides 4,5-diaryl-2-mercaptopyrimidine compounds in accordance with a general formula 1. A synthesis process comprises the steps of adding isoflavone and thiourea as reactant to a reaction kettle, adding a solvent and an appropriate amount of sodium hydroxide solution, controlling the temperature of a reaction solution, stirring and refluxing the reaction solution, enabling the reaction solution to react, obtaining a mixture of 4,5-diaryl-2-mercaptopyrimidine compounds and unreacted reactants, purifying the mixture through decompression, suction filtration and recrystallization and obtaining pure products of the compounds. The invention also provides a medicine with good anti-leukemia effects and a composition thereof containing a therapeutic effective amount of the synthesized compounds and a pharmaceutically acceptable carrier, as well as application of the synthesized compounds to the preparation of the anti-leukemia medicines.
EP2655355A1 New triazolylphenyl sulfonamides as serine/threonine kinase inhibitors The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A,X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
WO2009053697A1 Polymorphic forms of ( s ) -rotigotine hydrochloride The present invention is concerned with new polymorphic forms of rotigotine hydrochloride, processes of preparing the new polymorphic forms, pharmaceutical compositions containing the same, therapeutic uses thereof and methods of treatment employing the same.
CA2324848C Method of making camptothecin and camptothecin analogs Compounds of Formula I(see formula I) are made in accordance with the following scheme:(see formula II) (see formula III) (see formula IV) wherein R may be loweralkyl; R1 may be H, loweralkyl, loweralkoxy, or halo; R2, R3, R4, and R5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amide, hydrazine, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and Xare halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.
US7989442 (cis)-8-fluorodibenzo[b,f]pyrido[1,2-d]oxazepine-1-amine derivatives; contraception, hormone replacement therapy (HRT) or gynaecological disorders, adjuvant therapy in cancer The present invention provides new progesterone receptor modulators which are (cis)-8-fluorodibenzo[b,f]pyrido[1,2-d]oxazepine-1-amine compounds and uses thereof.
US20100093768 Agents for Reversing Epigenetic Silencing of Genes The present invention provides methods for discovering agents that are effective in reversing epigenetic silencing by inhibiting the interaction of methyl-binding (MBD) proteins with methylated genomic DNA. Also provided are methods for reactivating silenced genes having CpG island hypermethylation along with methods for treatment and prevention of diseases, such as cancer and sickle cell anemia, by administering an agent that modulates methyl-binding domain (MBD) protein-mediated transcriptional repression, thereby increasing gene transcription to prevent or treat disease. Additionally, compounds identified by the present invention useful for treatment and prevention of diseases, such as cancer and sickle cell anemia, are provided.
WO2007059950A3 Dry powder pharmaceutical formulations of purine a2a agonists The present invention provides a pharmaceutical dry powder composition comprising (i) a compound of formula (I): or a salt or solvate thereof in solid particulate form; (ii) one or more pharmaceutically acceptable particulate carriers; and (iii) one or more stabilising excipients of potential use in the treatment of inflammatory diseases such as asthma and chronic obstructive pulmonary disease.
USRE40259 side effects reduction; compounds active on the central nervous system; chronic and neuropathic pain, anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and hypnotic agents; 2-[4-(3-fluorobenzyloxy)benzylamino]-2-methylpropanamide The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents. In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain. Accordingly, one object of the present invention is to provide the use of a compound of formula (I) wherein: A is a —(CH2)m—, —(CH2)n—X— or —(CH2)v—O— group wherein m is an integer of 1 to 4, n is zero or an integer of 1 to 4, X is —S— or —NH—, and v is zero or an integer of 1 to 5; s is 1 or 2; R is a furyl, thienyl, or pyridyl ring or a phenyl ring optionally substituted by one or two substituents independently chosen from halogen, cyano, C1-C4 alkyl, C1-C4 alkoxy and trifluoromethyl; R1 is hydrogen or C1-C4 alkyl; one of R2 and R3 is hydrogen and the other is hydrogen or C1-C4 alkyl optionally substituted by hydroxy or phenyl; or R2 and R3 taken together with the carbon atom to which they are linked form a C3-C6 cycloalkyl ring; or R2 and R3 are both methyl; R4 is hydrogen or C1-C4 alkyl.
WO2006117370A1 4-PHENYL-5-OXO-l,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES AS MEDICAMENTS FOR THE TREATMENT OF INFERTILITY The invention relates to a 4-phenyl-5-oxo-l,4,5,6,7,8-hexahydroquinoline derivative according to Formula (I), wherein the substituents are defined as in the description, or a pharmaceutically salt thereof. The compounds of this invention are potent FSH receptor activators and may be used for treating fertility disorders in e.g. controlled ovarian hyperstimulation and IVF procedures.
US20080108627 9-[(3-hydroxy-5-methoxyphenyl)amino]-1,2-dihydrothieno[3,2-f]quinoline-8-carbonitrile 3,3-dioxide; protein tyrosine kinases inhibitor, especially erythropoetin-producing hepatoma amplified sequence (Eph) receptors antagonist; antitumor, angiogenesis inhibitor, neurodegenerative diseases The present invention relates to a quinoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).
US7485634 Methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
CN103393736A Pharmaceutical composition for treating alzheimer disease and preparation method as well as application thereof The invention discloses a pharmaceutical composition for treating alzheimer disease. The pharmaceutical composition comprises 24-60 parts by weight of nervonic acid and 48-90 parts by weight of panax notoginseng saponins. The pharmaceutical composition has an obvious treatment effect on the alzheimer disease and has no toxic or side effect. The invention also provides a preparation method as well as an application of the pharmaceutical composition.
US8207223 Pharmaceutical composition for treatment of diseases associated with decrease in bone mass comprising EP4 agonist as active ingredient A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).
US20120009130 Viral Therapy and Prophylaxis Using Nanotechnology Delivery Techniques The present disclosure provides compositions and methods of enhancing resistance to viral infections through targeted delivery of 5′PPP negative stranded siRNA via nanoparticles, specifically gold nanorods. The 5′PPP activates type I interferon through the signaling cascade providing a novel therapeutic and prophylactic for seasonal and pandemic influenza. The technology described herein also extends the findings to the use of nanoparticles for delivery of genetic material including but not limited to siRNA and microRNA to accomplish targeted nanoparticle based gene therapy.
CN101194909A Dropping pills containing gastrodine and method for preparing the same The invention provides an analgesic medicament, which particularly relates to a dripping pill which contains gastrodine and a process for preparation. The invention particularly relates to a dripping pill which contains acetyl gastrodine and a process for preparation. The invention overcomes the shortcomings of the prior dripping pills that pure natural degrees of findings which are used by the prior dripping pills are not high, and chemosynthesis findings which are commonly used are not in food additives catalogs of some countries, and tastes of the dripping pills are worse. The invention is a pharmaceutical preparation whose natural degree is higher, safety is stronger, and side effect is lower.
WO2010093788A2 Multiplex dicer substrate rna interference molecules having joining sequences The present invention is based, at least in part, upon the insight that compound DsiRNA agents can be generated using site-specific RNase H-cleavable double stranded nucleic acid double stranded nucleic acid regions to attach, e.g., one DsiRNA moiety to another DsiRNA moiety and/or one DsiRNA moiety to a functional group and/or payload. Because such double stranded nucleic acid joining sequences are site-specifically RNase H-cleavable, the bifunctional molecule is cleaved into DsiRNAs which bear terminal ends that orient dicer cleavage. The detrimental impact of administering a single double stranded nucleic acid RNAi agent of longer than 30- 35 nucleotides in length (e.g., provocation of interferon response) can be minimized, as once administered or delivered to a subject or RNase H-containing cell, RNase H cleavage produces a shortened, active DsiRNA agent(s). The invention also provides bifunctional DsiRNA agents that are joined by double stranded DNA extension joining sequences - such bifunctional DsiRNA agents joined by dsDNA sequences do not provoke RNase H cleavage.
US20050214378 Stealth lipid nanocapsules, methods for the preparation thereof and use thereof as a carrier for active principle(s) The present invention relates to stealth lipid nanocapsules comprising an essentially lipid core which is liquid or semi-liquid at ambient temperature, and an outer lipid envelope comprising at least one hydrophilic surfactant which is lipidic in nature, at least one lipophilic surfactant which is lipidic in nature and at least one amphiphilic derivative of poly(ethylene glycol), the molar mass of the poly(ethylene glycol) component of which is greater than or equal to 1000 g/mol, preferably greater than or equal to 2000 g/mol, to the methods for the preparation thereof and to the use thereof as a carrier for active principle(s).
US20100016213 Use of a diterpenoid compound for treating diabetes A method for lowering the plasma glucose level in a subject and for treating diabetes with a diterpenoid compound.
US20110124694 Bioavailable compositions of metaxalone and processes for producing the same Pharmaceutical compositions comprising metaxalone which demonstrate improved dissolution and bioavailability characteristics compared to the commercially available product, and methods of producing them are provided. In a preferred embodiment, a dosage form comprising metaxalone and at least one inactive powder excipient is bioequivalent to its commercially available counterpart (Skelaxin® 400-mg tablets) after oral administration to fasting or non-fasting human subjects, while at the same time displaying faster drug dissolution rates than the Skelaxin® tablets as demonstrated from three different dissolution tests. In another preferred embodiment, a dosage form comprising metaxalone, at least one inactive powder excipient and a nonvolatile liquid is significantly more bioavailable than the commercially available Skelaxin® 400-mg tablets after oral administration to fasting human subjects.
US7262212 Antitubercular agent; antibiotic against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria; e.g. (R)-2-methyl-6-nitro-2-(4-(4-(4-trifluoromethoxyphenoxy)piperidin-1-yl)phenoxymethyl)-2,3-dihydroimidazo(2,1-b)oxazole The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: wherein R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R2 represents a group —OR3 or the like, and R3 represents a hydrogen atom, C1-C6 alkyl group or the like, or R1 and —(CH2)nR2 may bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H): wherein R41 is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.
US20090018193 Essential fatty acids in the prevention of cardiovascular events The invention concerns the use of essential fatty acids with a high content in eicosapentaenoic acid ethyl ester (EPA) or docosahexaenoic acid ethyl ester (DHA) or a high concentration mixture thereof in the preparation of a medicament useful for preventing mortality, in particular due to sudden death, in patients who have suffered from a myocardial infarction.
US20130303496 Method Of Treating Vascular Lesions The present invention relates to the treatment of vascular lesions using low doses of an mTOR inhibitor together with a low dose of a glucocorticoid on an implantable medical device, wherein the treatment is particularly beneficial when the patient is a diabetic or is suffering from an abnormally long or diffuse lesion.
EP2484680A1 Useful Combinations of Monobactam Antibiotics with beta-Lac-tamase Inhibitors A pharmaceutical composition, comprising a combination of an antibiotically active compound of the formula I: with a β-lactamase inhibitor of one of the formulae II to XIII are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another β-lactamase inhibitor of one of the formulae II to XIII, particularly of formula V or formula VI.
CN101891674A 4-styryl pyridine compound and preparation method as well as application thereof The invention discloses a 4-styryl pyridine compound with the structural formula (1), wherein the R1 is X or B, the X is hydrogen or chlorine or bromine, and the B is 2-methyl-2-alcohol-3-butyne alkynyl, the R2 is W or Y or Z, the W is hydrogen, the Y is tert-butoxy-formyl, the Z is benzoyl or formal cyclopropane and the n is 2 or 3. The 4-styryl pyridine compound has increment inhibitory activity to K562 cells and can be used for preparing antineoplastic agents.
CN102309767A Soluble osthole clathrate, dispersing tablet and preparation method thereof The invention discloses a soluble osthole clathrate, a dispersing tablet and a preparation method thereof. Beta-cyclodextrin (beta-CD) is adopted as a carrier to prepare the osthole-beta-cyclodextrin clathrate (Ost-beta-CD), thus greatly raising the solubility and stability of osthole and reducing the irritation to gastrointestinal tract; simultaneously, by the selection of high-quality auxiliary materials, an osthole clathrate dispersing tablet which disintegrates rapidly and disperses uniformly is provided. The dispersing tablet can be swallowed and chewed, and can also be taken in dosages after being put into water and dispersed uniformly, especially suitable for elders, children and patients who have difficulty in swallowing solids. A preparation technology provided by the invention is adopted to raise the bioavailability of the hardly soluble medicament osthole and improve the curative effect of the medicament.
US20120244157 Use of tnf-alpha inhibitors for treating a nerve disorder mediated by nucleus pulposus The present invention relates to a method and a pharmaceutical composition for treatment of nerve disorders comprising administration of a therapeutically effective dosage of at least two substances selected from the group consisting of TNF inhibitors, IL-1 inhibitors, IL-6 inhibitors, IL-8 inhibitors, FAS inhibitors, FAS ligand inhibitors, and IFN-gamma inhibitors. Preferably, at least one of the substances is a TNF inhibitor.
CN101036687A Gypenosides dropping pills and the method for preparing the same The invention relates to a gypenoside pill and a method for preparing the same. The gypenoside pill comprises a gypenoside as an active ingredient and polyethyleneglycol 4000 and polyethyleneglycol 400 as a substrate. The preparing method includes: heating proper polyethyleneglycol 4000 to fuse, then adding suitable polyethyleneglycol 400 and gypenoside, mixing uniformly the mixture to drop the same into a coolant, thus the pill is obtained. The pill formulation without defects of the existing granular formulation is applicable to hyperlipoidemia and is capable of descending the blood fattiness, strengthening the spleen, benefiting qi and to harmonizing blood, removing phlegm and blood stasis.
US20100144675 Regulation of sGC Function by Corrin Derivatives We disclose a method of activating soluble guanylyl cyclase (sGC) in a patient, comprising administering to the patient a composition comprising a corrin and a pharmaceutically-acceptable carrier. We also disclose a composition, comprising a corrin, an NO-independent sGC activator selected from the group consisting of BAY 41-2272, BAY 58-2667, HMR1766, YC-I, and S3448, and a pharmaceutically-acceptable carrier.
CN102440971A Iloperidone orally disintegrating tablet The invention relates to an iloperidone orally disintegrating tablet, which is characterized in that: 1) the grain size D of the iloperidone is less than or equal to 90 and more than or equal to 30 mum; 2) the proportion of water-solubility components in the tablet is more than or equal to 50%; and 3) the orally disintegrating tablet can be disintegrated when meeting spittle in an oral cavity.
US20110003834 Production method and production apparatus for a high theobromine-containing composition An object is to provide a method for producing a high theobromine-containing composition effectively in a simple way. The method for producing a theobromine-containing composition comprises: (a) performing an extraction of a theobromine-containing plant or a processed product thereof with a solvent, to obtain a crude theobromine extract; (b) applying the crude theobromine extract to a cation exchange resin subjected in advance to hydrogen ion substitution, to allow an adsorption of theobromine onto the cation exchange resin; and (c) passing a solvent containing no ionic substance through the cation exchange resin subsequently to the step (b), to obtain a theobromine eluate.
US20060120993 Treatment of lesions of the soft tissues The invented remedy allows cleaning up the area from necrotic tissues and facilitating reduced perifocal oedema and infiltration as well as lessening pain syndrome during suppurative inflammation diseases. The remedy can be applied both in the hospital and field settings.
US20100183593 Gene Polymorphisms Predictive for Dual TKI Therapy The invention provides compositions and methods for determining the likelihood of successful treatment with dual therapy such as lapatinib. The methods comprise determining the genomic polymorphism or expression level of a gene present in a predetermined region of a gene of interest and correlating the polymorphism or expression level to the predictive response. Patients identified as likely responsive are then treated with the appropriate therapy.
CN102920696A Application of mangiferin compound or mango extraction as pancreatic lipase inhibitor and to preparation of medicament or food for preventing and treating obesity The invention provides an application of a mangiferin compound with a structure shown as a formula I as a pancreatic lipase inhibitor, an application of a mango extract containing the mangiferin compound with the structure shown as the formula I as a pancreatic lipase inhibitor, and an application of the mangiferin compound with the structure shown as the formula I or the mango extract containing the mangiferin compound with the structure shown as the formula I to preparation of a medicament or a food for treating and/or preventing obesity, and provides an application of the mangiferin compound with the structure shown as the formula I or the mango extract containing the mangiferin compound with the structure shown as the formula I to preparation of a medicament or a food for treating and/or preventing obesity. The mangiferin compound has the function of inhibiting the activity of pancreatic lipase, so that the occurrence of obesity can be avoided by inhibiting the accumulation of in-vivo fat. Meanwhile, the mangiferin compound has wide physiological activity, so that side effects on human bodies caused by the conventional weight-losing product can be avoided.
CN103373981A Application of oxygen heterocycle containing sulfanilamide derivative The invention relates to a sulfanilamide derivative which is characterized in that the derivative has the following formula, in which n is 1, 2, 3, and R is a radical. The sulfanilamide derivative provided by the invention has remarkable inhibiting effect on human breast cancer (MCF-7), so that the sulfanilamide derivative provided by the invention can be applied to preparing antitumor medicines. The invention discloses a preparation method of the sulfanilamide derivative.
US20080058330 Compounds and Combinations Thereof for Inhibiting Beta-Amyloid Production and Methods of Use Thereof Provided are compounds which can be used in combination for treating diseases associated with a condition associated with cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods of treating or reducing the risk of developing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of compounds which in combination can decrease β-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of the compounds.
CN101766816B Dipolar molecule-modified mesoporous silicon material, preparation and application thereof The invention relates to a dipolar molecule-modified mesoporous silicon material, preparation and application thereof. The dipolar molecule-modified mesoporous silicon material is prepared by coupling a dipolar molecule with silane end group graft and mesoporous silicon with a pore structure through a silicon-oxygen bond. A drug control and release system prepared by taking the dipolar molecule-modified mesoporous silicon material as a carrier can realize continuous control and release of guest molecules in the system through adjusting the applied electric field. The dielectrical property test shows that the drug control and release system has excellent electric field responsiveness and can be recycled through simple cleaning treatment after drug release.
US20110294864 Aqueous coacervate compositions suitable for making powders and water-soluble formulations of biologically-active agents Aqueous gel-free two-phase coacervate compositions including a coacervate phase and an equilibrium water phase, comprising a mixture of: (a) a poorly water-soluble bio-active agent, (b) a tensio-active system consisting of non-ionic tensio-active agents, (c) one or more water-soluble carriers for said poorly water-soluble bio-active agent, said carriers being selected from the group consisting of maltodextrins and polyols, and (d) water. Such coacervate compositions may be dried into solid dosage forms from which rapid release of the bio-active agent can be obtained.
WO2011016468A1 Benzyl piperidine compound Provided is a new serotonin-reuptake inhibitor that exhibits affinity for serotonin-1A receptors. Said serotonin-reuptake inhibitor is a compound represented by formula (1) or a pharmacologically-permitted salt thereof. In the formula, R1 represents a hydrogen atom, a 2-hydroxyethyl group, or a 2-methoxyethyl group. R2 represents one of the following bonded to a methylene group which is bonded to a piperidine ring: a chlorine atom bonded in a p-position; a bromine atom bonded in a p-position; a methyl group bonded in a p-position; a chlorine atom bonded in an m-position; or a bromine atom bonded in an m-position. Either Y1 represents a hydrogen atom and Y2 represents a hydrogen atom or a hydroxyl group, or Y1 and Y2 together represent an oxo group. Z represents a group represented by one of the following formulas: formula (3-1-1), formula (3-1-2), formula (3-2-1), formula (3-2-2), formula (3-3-1), formula (3-3-2), formula (3-4-1), or formula (3-4-2). However, if R1 represents a 2-hydroxyethyl group or a 2-methoxyethyl group and Y1 and Y2 both simultaneously represent hydrogen atoms, then Z represents a group represented by one of the following formulas: formula (3-1-2), formula (3-2-1), formula (3-2-2), formula (3-3-1), formula (3-3-2), formula (3-4-1), or formula (3-4-2).
US20110250293 Present invention relates to compositions and methods for the treatment of topical skin conditions, comprising of shea butter, jojoba oil, dihydrogen oxide, Stearic acid, Anhydrous Magnesium Sulphate, Zinc Oxide, Glycerin and a suitable amount of a Pharmaceutically acceptable carrier, one or both of the following: Cocoa butter and or petroleum jelly. The present invention relates to compositions and methods for the treatment of topical skin conditions, comprising of shea butter, jojoba oil, dihydrogen oxide, Stearic acid, Anhydrous Magnesium Sulphate, Zinc Oxide, Glycerin and a suitable amount of a pharmaceutically acceptable carrier, one or both of the following: Cocoa butter and or petroleum jelly.
CN101096359B Polyaryl substituted methane oxygen or silica radical guanidine compound and preparation method and usage thereof The invention discloses a compound as general formula (I), making method of the compound and application as nerve adjusting peptide U receptor modifier in the cardiovascular disease, immune system disease, metabolic disease (such as obesity)and cancer treatments.
CN101481397B Novel kanamycin A derivative, and preparation and use thereof The invention discloses a new kanamycin A derivative, that is, a compound as shown in formula (I). The new kanamycin A derivative has antibacterial activity, and detailed definitions of various groups are shown in the specification. In addition, the invention discloses a preparation method of the derivative and a pharmaceutical composition containing the derivative.
CN103463199A Composition for subcutaneous tissue trauma A composition for subcutaneous tissue trauma comprises: by weight percentage, 0.3-0.4% of lotus root powder, 0.1-0.2% of an antimicrobial agent and the balance of paraffin oil. The composition for the subcutaneous tissue trauma can promote flesh granulation proliferation and forming at a traumatic part, and can help traumatic part recovery and eliminate traumatic part scars.
WO2010005585A3 4-aminoquinazoline prodrugs This invention relates to prodrugs of 4-aminoquinazoline compounds, and to pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER2.
CA2847915A1 Pharmaceutical combinations including anti-inflammatory and antioxidant conjugates useful for treating metabolic disorders One aspect of the present invention is a pharmaceutical combination comprising (a) an anti-inflammatory agent/anti-oxidant agent conjugate; and (b) an insulin secretogogue, an insulin sensitizer, an alpha-glucosidase inhibitor, a peptide analog, or a combination thereof. Another aspect of the invention relates to methods of treating metabolic disorders with such conjugates.
WO2007117180A1 Azaheterocycles, combinatory library, focused library, pharmaceutical composition and methods for the production thereof The invention relates to novel azaheterocycles of interest as potential physiologically active substances (agonists, antagonists, receptor modulators, ferment inhibitors, oncolytics, antibacterial and antiparasitic agent etc.), to combinatory and focused libraries comprising novel azaheterocycles of a pharmaceutical composition containing said novel azaheterocycles in the form of an active substance and to methods for the production and the use thereof. Said novel azaheterocycles are of general formula (1), wherein W is an azaheterocycle which comprises 6-12 atoms, is optionally annelated, has at least one C5-C7 carbocycle and/or heterocycle, and also comprises at least one of heteroatoms and is selected from an O, S or N group; R1ais an aminogroup substituent, apart from hydrogen, preferably C1-C6 alkyl, aryl or heterocycle comprising at least one of heteroatoms selected from theO, S or N group; Rb is a carbamoyl group -C(O)NHRa in which Ra is the aminogroup substituent, apart from hydrogen; Rc is a cyclic system substituent, preferably C1-C6 alkyl, alkyl, aryl or heterocycle comprising at least one of heteroatoms selected from theO, S or N group, or Rb and Rc together form an amino-cyano-methylen [(=C(NH2)CN] group.
WO2010150564A1 Benzaldehyde compound A compound represented by formula (I), which has an effect of promoting the folding of a mutant rhodopsin and is useful as the active ingredient of a drug for preventing and/or treating retinitis pigmentosa, or a salt thereof [in formula (I), R1 represents an aldehyde group; R2 and R3 represent a hydrogen atom, a hydroxyl group, an alkyl group, etc.; L1, L2 and L3 represent -C(R4)(R5)- (wherein R4 and R5 represent a hydrogen atom, a hydroxyl group, a halogen atom, etc.), -O-, -N(R6)- (wherein R6 represents a hydrogen atom or an alkyl group), -C(=Q)- (wherein =Q represents =O, =S, etc.), or =C(R8)(R9) (wherein R8 and R9 represent a hydrogen atom or an alkyl group); X represents -CH2-, -CH2-CH2-, etc.; and Y and Z represent -O-, -CH2-, etc.].
US20090203784 Treatment regimen for n-myc, c-myc, and l-myc amplified and overexpressed tumors The present invention relates to methods and compositions for treating diseases. More specifically, the present invention relates to the administration of multiple drugs as part of a treatment of disease. Specific embodiments of the invention relate to a treatment regimen for neuroblastomas and other N-MYC, c-MYC, and L-MYC amplified and overexpressed tumors, comprising administering multiple therapeutic compounds like DFMO, SAM486A, a verinoid and a cytotoxic drug and placing the patient on a low polyamine diet and/or providing the patient with a polyamine limiting dietary supplement.
WO2008153443A1 Method for bio-controllable photo-dynamic therapy The invention relates to medicine. In order to increase the effectiveness of the bio-controllable photo-dynamic therapy by improving the accuracy of diagnosis of deeply located tumors, to accelerate a rehabilitation period and to increase the selectivity of the laser action, one of the variants of the inventive method consists in diagnosing the tumor and metastasis sites, including the early stages of development thereof, in intravenously or otherwise injecting a photosensitiser and in producing the biochoronotherapy-correlated laser action, wherein the hardware-software 'Constellation' system is used during diagnosis for refining the tumour site and the laser action is carried out by irradiating at a wave length of 660±20 nm, a pulse repetition rate of 22,5±2 kHz, a pulse length of 70±30 ns and a power density of 0.1-0.5 W/cm2.
US20070243231 Use of Whey Permeate for the Treatment of Metabolic Syndrome The invention relates to the use of whey permeate, preferably sweet whey permeate and more preferably hydrolysed or partially-hydrolysed sweet whey permeate for the production of a pharmaceutical composition for prophylaxis or treatment of symptoms of metabolic syndrome, type-2 diabetes and secondary diseases, said composition being provided for a mammal.
CN101766618A New use of pitavastatin calcium and drug aiming at new use The invention relates to a new use of pitavastatin calcium and a drug aiming at the new use, in particular to a new use of pitavastatin calcium in preparing drugs for curing or preventing hyperlipidemia plus cerebral infarction, belonging to the pharmaceutical field. The drug contains 1-5 percent of active ingredient pitavastatin calcium by weight percent and auxiliary materials. Pitavastatin calcium can obviously improve hemorheological index of patients, can effectively relieve the hyperlipidemia manifestations of patients and can improve neurological functions, thereby being beneficial to overall restoration of the patients from illness.
EP1526856B1 Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy The present invention relates to a method of treating or preventing estrogen-sensitive tumours in a mammal, said method comprising the administration of a therapeutically effective amount of an estrogenic component to said mammal, wherein the estrogenic component is selected from the group consisting of: substances represented by the following formula (I) in which formula R1, R2, R3, R4, independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. The estrogenic component according to the invention does not have undesirable proliferative effects on breast and/or endometrial tissue and displays sufficient estrogenicity to prevent that its administration will lead to hypoestrogenism and/or climacteric complaints. Other aspects of the invention relate to pharmaceutical compositions, drug delivery systems and kits comprising the aforementioned estrogenic component in combination with an estrogen suppressant.
DE102006024911A1 Solubilizate of plant extract that contains active agent, useful as additive for e.g. cosmetics, pharmaceuticals and foods, includes water and emulsifier Solubilizate (A) of a plant extract (B), which contains physiologically or pharmaceutically active agents (I), comprises about (by weight) 10-30% (B); 4-35% water (deionized, demineralized or distilled, one or more times) and 55-75% of an emulsifier (II) with hydrophilic-lipophilic balance (HLB) 9-16. An independent claim is included for a method for preparing (A).
US8669293 Method and compositions for preventing hormone induced adverse effects A method for preventing the adverse effects which may he associated with the administration of at least one hormone to a subject without detectable cancer comprising administering to such subject at least one carotenoid. The method of the instant invention can be utilized to prevent a variety of adverse effects associated with the administration of hormones, including for example, an increased risk for developing cancer. The instantly claimed method prevents such adverse effects without inhibiting the beneficial activity of the hormone. Further provided by the present invention are compositions which are useful for preventing the adverse effects associated with the administration of hormones. The compositions of the instant invention may be in unit dosage form suitable for daily administration to a human.
US20110319456 Benzoarylureido compounds, and composition for prevention or treatment of neurodegenerative brain disease containing the same Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.
WO2010012153A1 Phlorizin derivatives and their preparation and application Phlorizin derivatives of formula (I), their preparation and their use for manufacture of pharmaceutical compositions. The said compounds exhibit SGLT2 inhibitory activity and can be used to treat metabolic diseases such as diabetes and its complication.
EP2606893A1 Sulphonylaminopyrrolidinone derivatives, their preparation and their therapeutic application The invention relates to new sulphonylaminopyrrolidinone compounds having antithrombotic activity which, in particular, inhibit blood clotting factor IXa and/ or factor Xa, to processes for their preparation and to use thereof as drugs.
EP1575591A1 Heterocycles and uses thereof Compounds of the following formula are disclosed: wherein RB is a substituted or unsubstituted aryl or heteroaryl moiety; at least one of RU and RL is a phosphorus-containing moiety, J, and the other of RU and RL is independently chosen from H; halogen; -CN; -N02; -J; -SO2R; -S02NRR'; or -ZRJ, wherein each occurrence of Z is independently -0-, -S- or -NR- and each occurrence of RJ is independently -R, -COR, -COOR or -CONRR.
CN102304191A Method for extracting crude polysaccharide from waste internal organs of sea worms The invention discloses a method for extracting crude polysaccharide from waste internal organs of sea worms, which belongs to the field of recycling of agricultural waste and particularly relates to a method for extracting crude polysaccharide from waste internal organs of sea worms. The invention provides a method for extracting crude polysaccharide from waste internal organs of sea worms, which is simple in operation, high in yield and high in product activity. In the invention, crude polysaccharide is obtained by using waste organs of sea worms as raw materials and by impurity removing, crushing, defatting, enzymolysis, deproteinization, precipitating and freeze-drying.
EP1762239A1 Lofexidine for intraspinal administration The present invention provides use of lofexidine or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for intraspinal administration to provide analgesia.
WO2014142757A1 Hybrid nanomaterial of graphene oxide nanomaterial and cationic quaternized chitosan A hybrid nanomaterial consisting of graphene oxide (GO) nanomaterial covalently conjugated to cationic quaternized chitosan is provided. Method of preparing the hybrid nanomaterial, an antimicrobial composition containing the hybrid nanomateiral, and use of the antimicrobial composition in inhibiting growth of microorganisms in an environment are also provided.
US7737127 2-propynyl adenosine analogs having A2A agonist activity and compositions thereof The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.
US20100104651 Pharmaceutical Compositions Containing Diacerein A once-daily controlled-release formulation of diacerein for treating inflammatory or autoimmune diseases or their complications, with reduced adverse side effects and methods of treating such diseases are disclosed.
CN101244052A Oral administration solid preparation containing component for reducing blood fat The invention relates to an oral drug preparation containing pravastatin, in particular to an oral solid formulation with reinforced effect of pravastatin, which comprises effective amount of pravastatin and pharmaceutical adjuvant, wherein the pharmaceutical adjuvant comprises an enwrap agent; the weight proportion of the pravastatin and the enwrap agent ranges from 1: 0.2 to 1: 10. The oral drug has the advantages of quick effects, reinforced active components and easy drug taking without uncomfortable feeling.
US20090082298 Methods for producing microRNAs The invention relates to recombinant vectors for inducible and/or tissue specific expression of double-stranded RNA molecules that interfere with the expression of a target gene. In certain embodiments, the invention relates to the use of Tet (tetracycline)-responsive RNA Polymerase II (Pol II) promoters (e.g., TetON or TetOFF) to direct inducible knockdown in certain cells of an integrated or an endogenous gene, such as p53. The invention also relates to a method for producing transgenic animals (e.g., mice) expressing inducible (such as tetracycline-regulated), reversible, and/or tissue-specific double-stranded RNA molecules that interfere with the expression of a target gene.
US20100323000 Method and process for preparing cardiolipin The invention provides novel methods for preparing cardiolipin and cardiolipin analogs having varying fatty acid chain lengths, particularly 1,1′,2,2′-tetramyristoyl cardiolipin. The methods comprise reacting a starting compound, such as a 1,2-O-sn-diacylglycerol and a 2-protected glycerol, with a phosphoramidite reagent to produce a protected cardiolipin, which is deprotected to prepare cardiolipin. The cardiolipin and cardiolipin analogs may be prepared in the presence of an activator, such as pyridinium trifluororacetate. The methods of the present invention are used to prepare cardiolipin and cardiolipin analogs in large quantities. The cardiolipin prepared by the present methods can be incorporated into liposomes which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays.
CN102838567A Benzenesulfonyl piperazine compounds or benzoyl piperazine compounds, preparation methods and uses thereof The present invention relates to benzenesulfonyl piperazine compounds represented by a formula I or benzoyl piperazine compounds represented by a formula II, or pharmaceutically acceptable salts, solvates, stereoisomers or precursor drugs thereof, wherein various symbols are described in an instruction. The present invention further relates to preparation methods for the compounds, uses of the compounds in preparation of drugs for treatment and/or prevention of tumors and/or cancers, methods for treatment and/or prevention of tumors and/or cancers by using the compounds, and drug compositions containing the compounds having an effective treatment and/or prevention amount. The compounds of the present invention have characteristics of effective anticancer activity and low toxicity.
CN1850021A Use of conjugated linoleic acid and its derivative for deep nourishing skin The present invention relates to a conjugated linobeic acid and its derivative skin care preparation and its application. Said application includes: eliminating skin wrinkles, raising skin elasticity, whitening skin, resisting inflammation, moistening skin, tonifying skin, resisting allergic dermatitis and curing dermatesis, etc.
CN102552749A Chewable tablets for treating hand-foot-and-mouth diseases and preparation method thereof The invention discloses chewable tablets for treating hand-foot-and-mouth diseases and a preparation method thereof. The chewable tablets are characterized by comprising the following raw materials: greater celandine herb, lophatherum, leontice root, stir-fried lablab bean, common bombax flower, coix seed, hawthorn fruit, lalang grass rhizome, kaolin powder and a flavoring agent. The preparation method comprises the following steps of: performing water extraction on the greater celandine herb, the lophatherum, the leontice root, the stir-fried lablab bean, the common bombax flower, the coix seed, the hawthorn fruit and the lalang grass rhizome, and concentrating filtrate under reduced pressure to form thick extract; and drying the thick extract under the reduced pressure and crushing to obtain dry extract powder, adding the flavoring agent, mixing uniformly, granulating, adding the kaolin powder, and tabletting. Clinical application proves that the chewable tablets can treat the hand-foot-and-mouth diseases effectively and are worthy of clinical application and popularization.
US20100168184 Small molecule bcl-x1/bcl-2 binding inhibitors Bcl-xL/Bcl-2 binding inhibitors useful in the treatment of unwanted proliferating cells, including cancers and precancers, in subjects in need of such treatment. Also provided are methods of treating a subject having unwanted proliferating cells comprising administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject in need of such treatment. Also provided are methods of preventing the proliferation of unwanted proliferating cells, such as cancers and precancers, in a subject comprising the step of administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject at risk of developing a condition characterized by unwanted proliferating cells.
CN1857198A Tumor treating methyl cantharidimide injection and freeze dried powder for injection and their preparing process The present invention relates to a kind of intravenous dripped injection and freeze dried powder for injection of methyl cantharidimide with high anticancer and leukocyte increasing effects. The injection and the freeze dried powder for injection are prepared through dissolving methyl cantharidimide in compound solvent of propylene glycol, alcohol, glycerin and polyethylene glycol, compounding material, filtering, filling or freeze drying, sterilizing and packing. As one kind of broad antitumor medicine, the present invention is suitable for treating primary liver cancer, lung cancer, osophagus caner and other tumors and may be also used in treating hepatitis and hepatocirrhosis.
WO2012084267A1 Derivatives of englerin for the treatment of cancer The present invention relates to compounds of the general Formula (I), which show a specific activity against cancer cell lines, the use of these compounds for prophylaxis and treatment of cancer as well as to pharmaceutical compositions containing at least one compound of general formula (I).
WO2009093264A2 Pharmaceutical combinations comprising specified age breaker and further drugs, i.a. antihypertensive drugs, antidiabetic drugs etc. The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and/or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.
WO2007076085A2 Fused pyrimidones and thiopyrimidones, and uses thereof Compounds represented by Structural Formula (I): are useful, for example, in the effective killing or reduction in rate of proliferation of cancer cells, such as in patients suffering from cancer. In addition to the compounds themselves, the invention provides pharmaceutical compositions of the compounds and method of treatment using the compounds.
CN1969971A Transdermal absorption formulation of total alkaloid of common monkshood root and preparation process thereof The invention discloses a frame type percutaneous absorption externally-used preparation and process for preparing it, which comprises four portions of a storage layer, an adhesive layer, a back lining layer and a protection layer, wherein the storage layer comprises the following constituents (by weight ratio): Ligusticum wallichii alkaloid extract 7.5-12 parts, frame material 50-60 parts, methyl glycol 7-15 parts, azone 0.5-3 parts, and thickening agent 0-5 parts, other ingredients 5-35 parts. The preparation can be used for treating rheumatic and rheumatoid arthritis.
US20100119555 Methods and Compositions for the Treatment and Diagnosis of Cancer The invention provides methods of treatment of prion disease, cancers and other conditions, the methods comprising administration of an anti-Candida agent. Also disclosed are methods of diagnosing prion disease and cancers, said methods based on the determination of the presence of Candida infection, in particular systemic candidiasis.
CN103467391A Diaryl methyl piperazine compounds containing saturated nitrogen heterocyclic amide and application thereof The invention discloses substituted diaryl methyl piperazine compounds containing saturated nitrogen heterocyclic amide, or pharmaceutically acceptable esters, or pharmaceutically acceptable salts thereof. The compounds provided by the invention are delta opiate receptor agonists which can be used for treating Parkinsonism; compared with the existing diaryl methyl piperazine delta receptor agonists, such as BW373U86 and SNC80, the original N-diethyl amide is substituted by saturated nitrogen heterocyclic amide structural fragments with better metabolic stability in the compounds provided by the invention; the metabolic stability can be increased expectedly; the treatment effect of the compounds is well played.
US20100099755 Chemotherapeutic flavonoids, and syntheses thereof Substituted flavonoid compounds, and pharmaceutical formulations of flavonoid compounds are described. Also described are processes for preparing flavonid compounds, as are methods for treating cancer in mammals using the described flavonoid compounds or pharmaceutical formulations thereof.
US20080095800 Eliciting HCV-specific antibodies Described herein is a method of eliciting antibodies and neutralizing of binding antibodies against a hepatitis C virus (HCV) E1E2 or E2 antigen using HCV E2 or HCV E1E2 polypeptides and/or HCV E2 or E1E2 polynucleotides. Elicitation of anti-E2 antibodies and anti-E2 NOB antibodies can be used, inter alia, to provide model systems to optimize anti-E2 antibody responses and/or anti-E2 NOB antibody responses to HCV and to provide prophylactic or therapeutic treatment against HCV infection.
CN101959557A 2-aminoquinolines as 5-HT5A receptor antagonists The present invention is concerned with 2-Aminoquinoline derivatives as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders. In particular, the present invention is concerned with compounds of the general formula (I) wherein R and R are as described herein.
US20110178080 Melanocortin Receptor-Specific Spiro-Piperidine Compounds Melanocortin receptor-specific compounds of formula I below: wherein the variables are as defined in the specification, and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders.
WO2010025589A1 Long acting curcumine derivates and preparation method thereof The present invention provides long acting curcumine derivates and preparation method and pharmaceutical use thereof. The said curcumine derivates have the following structure, wherein the R1 and R2 is hydrogen or methoxyl, R3 and R4 is C1-C50 alkyl group independently. The delayed release effect of curcumine derivates in the present invention is superior to curcuminoids, and the said derivates has high bioavailability and pharmacological activity, and can treat depression and cancer.
US20110294879 Method of treatment of fragile x syndrome, down's syndrome, autism and related disorders Disclosed herein are methods of treating fragile X syndrome, fragile X-associated tremor/ataxia syndrome, Down's syndrome and/or autism, comprising administering a prodrug of acamprosate to a subject suffering therefrom, wherein, in certain embodiments, the acamprosate prodrugs comprise compounds of Formula (I).
WO2012171974A1 Tadalafil for the treatment of dementia The present invention relates to tadalafil, pharmaceutically acceptable salts and solvates thereof, for use in the prevention or treatment of dementia and Alzheimer's disease in a geriatric patient, wherein tadalafil is administered at a dose of 0.01-9 mg/day. The present invention also relates to the use of tadalafil, pharmaceutically acceptable salts and solvates thereof, for the manufacture of a medicament for the prevention or treatment of dementia and Alzheimer's disease in a geriatric patient, wherein tadalafil is administered at a dose of 0.01-9 mg/day. These uses of tadalafil comprise the administration to a geriatric patient of an amount of 0.01-9 mg/day effective to prevent or combat dementia and Alzheimer's disease. The invention also relates to a method of preventing or treating dementia and Alzheimer's disease in a geriatric patient, comprising administering to said patient an effective amount of tadalafil, wherein tadalafil is administered at a dose of 0.01-9 mg/day.
WO2007072497A3 Stabilized pharmaceutical composition of pramipexole and method of preparation thereof Stabilized pharmaceutical compositions comprising pramipexole or pharmaceutically acceptable salts thereof and one or more dextrins and to methods of preparation of the same. The said stabilized composition is in form of tablets comprising pramipexole dihydrochloride, ß-cyclodextrin and one or more pharmaceutically acceptable excipients. A process for preparing the stabilized tablet composition, the process comprising dissolving pramipexole dihydrochloride along with polyvinyl pyrrolidone in suitable solvent; granulating blend of cyclodextrin and other excipients with above solution as granulating fluid; drying of above formed granules; lubricating granules with glidants and anti-adherents; compressing granules using suitable tablet equipment. A further process of preparing a stabilized tablet composition the process comprising preparing pramipexole dihydrochloride - ß-cyclodextrin inclusion complex; admixing prepared inclusion complex with other excipients; granulating using either dry granulation process or wet granulation process or direct compression ; drying, sifting and lubricating, formed granules; compressing granules using suitable tablet equipment to form tablet. A method of packaging the stabilized pharmaceutical composition comprising including oxygen absorbers or inert gas in the packaging system comprising the composition.
US20090082306 Deuterium-enriched telbivudine The present application describes deuterium-enriched telbivudine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2011044742A1 Medicaments for inhibiting thrombosis The present invention provides a medicament for inhibiting thrombosis. The active components of the medicament of the present invention are triflusal and clopidogrel bisulfate. The quality ratio of triflusal to clopidogrel bisulfate is (100-650):(30-150), preferably (1-20):1, more preferably (3-6):1, and most preferably 3:1 or 6:1.
EP2253327A1 Pharmaceutical composition containing a compound having angiotensin II antagonistic activity in combination with another compound A pharmaceutical composition comprising (+)-1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H -benzimidazole-7-carboxylate, 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H -benzimidazole-7-carboxylic acid, 2-ethoxy-1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)bi phenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid, or a salt thereof, in combination with at least one species selected from the group consisting of: - 2,4-oxazolidinedione derivative or a salt thereof; - valiolamine derivative or a salt thereof and acarbose or a salt thereof; - indane derivative; - N-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-L-alanyl]-N-(indan-2-yl)glycine or a salt thereof; and - (+)-3R,5S-erythro-(E)-7-[4-(4-fluorophenyl)-2,6-diisopropyl-5-methoxymethylpyridin-3-yl]-3,5-dihydroxyhept -6-enoic acid or a salt thereof.
EP2762480A1 Oxazolidinone antibiotics containing fused ring The present invention relates to a fused ring-containing oxazolidinone compound shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, A, B and C are as defined in the description. The present invention further relates to a method for preparing the compound, a pharmaceutical composition and a pharmaceutical formulation comprising the compound, and a use of the compound for the manufacture of a medicament for the treatment and/or prevention of infectious diseases and a use for the treatment and/or prevention of infectious diseases.
WO2012099453A1 Pyrrolothiazole containing curcumin compounds Accordingly, the invention discloses compounds of pyrrolothiazole moiety containing with mono bis substituted curcumin molecules which improves solubility of curcumin. The invention also discloses the method in synthesizing these compounds wherein the steps includes mixing curcumin, isatin derivatives or ninhydrin and thioproline (thiazolidine-4-carboxylic acid) in 20 mL methanol. The mixture was then refiuxed with a solvent on a water bath and excess solvent was removed under vacuum. The residue subjected to flash column chromatography using petroleum ether: ethyl acetate mixture (4:1) as eluent to afford the product. The ratio for curcumin: isatin derivative/ninhydrin:thioproline (thiazolidine-4-carboxylic acid) is 1:1:2 and 1:2:4.
CN101879141A Taste-masking tilmicosin gastric-soluble particle preparation The invention relates to a taste-masking tilmicosin gastric-soluble particle preparation, in particular to a gastric-soluble particle preparation consisting of a gastric-soluble coating material, a high-polymer carrier, a disintegrating agent and the like and aims to solve the problem of poor palatability of tilmicosin.
WO2004080964A8 Indole derivatives useful for the treatment of diseases The invention relates to indole derivatives of formula (I) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
US20110311512 Genetic Variants Underlying Human Cognition and Methods of Use Thereof as Diagnostic and Therapeutic Targets Compositions and methods for the detection and treatment of neurological disorders, including ASD, are provided.
CN101891702B Crystal of febuxostat, preparation method and application in medicaments The invention relates to a crystal (type M) of febuxostat, a preparation method and an application in medicaments. The reflected angle 2theta of the crystal X-ray powder diffraction pattern has characteristic absorption peak at about 2.95 degrees, 5.84 degrees, 11.19 degrees, 14.04 degrees, 14.54 degrees, 16.75 degrees, 18.47 degrees, 20.81 degrees, 22.72 degrees, 24.34 degrees and 25.62 degrees,wherein the reflected angle 2theta has three strongest peaks at 11.19 degrees, 2.98 degrees and 5.84 degrees; in an infrared spectrum pattern, the characteristic absorption peak occurs at about 3425cm<1>, 2964cm<1>, 2873cm<1>, 1689cm<1>, 835cm<1>, 815cm<1>, 765cm<1> and 729cm<1>; the particle diameter measured with a laser diffraction method ranges from 0.5 mu m to 50 mu m, the counting particle diameter D90 is less than 40 mu m and the average particle diameter is less than 20 mu m. The crystal can be obtained by recrystalling the febuxostat with toluene; the crystal and pharmaceutically acceptable auxiliary parts can form the useable corresponding medicinal preparation with satisfactory dissolving rate; the dissolution of a tablet in phosphate buffer solution medium with the pH value of7.2 is greater than or equal to 45% within five minutes and greater than or equal to 95% within 35 minutes.
CN103626680A Diethylstilbestrol disulfamate derivatives and medicinal uses thereof The invention belongs to the fields of the organic chemistry and the medicine synthesis, and concretely relates to diethylstilbestrol disulfamate compounds having a structure represented by formula 1. The diethylstilbestrol disulfamate compounds comprise hexestrol disulfamate, 3-diethylstilbestrol disulfamate, 2-diethylstilbestrol disulfamate, 2,4-diethylstilbestrol disulfamate and derivatives obtained after substituting 3'-position of the above compounds by different substituent groups. Biological activity determination results of human umbilical vein endothelial cell model drug sieving experiments and series hormone-dependent tumor cell strain model drug sieving tests show that the compounds can inhibit the growth of HUVEC and all tumor cell strains, have a substantial newborn blood vessel inhibition effect and a substantial steroid sulfatase inhibition activity, and can be used for preparing tumor treatment medicines.
WO2009100929A1 Pharmaceutical compositions comprising n-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2- dihydro-2-oxo-3h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide The present invention relates to a pharmaceutical composition comprising: N-[2-(diethylamino) ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene) methyl] -2,4-dimethyl-1H-pyrrole-3-carboxamide or a pharmaceutically acceptable salt thereof as active pharmaceutical ingredient, wherein the active pharmaceutical ingredient is present in amorphous or partially amorphous form.
US20070166413 Cholestrol-reducing agent containing an n-3 fatty acid This invention relates to a cholesterol-reducing active substance combination containing at least one cholesterol-reducing carob product, particularly water-insoluble carob fibers, at least one n-3 fatty acid and at least one cholesterol-reducing active substance. The invention also relates to a method for producing active substance combinations of this type and to the use thereof.
CN1895247A Buccale tablet preparation and its making method A medicine in the form of buccal lozenge or oral paster for treating the oral diseases caused by anaerobic bacteria, such as gingivitis, periodontitis, periocoronitis, oral mucosa ulcer, etc, is prepared from ornidazole, skeleton, filler, flavouring, odor mask, lubricant and moistening agent proportionally.
EP1795182A1 Liposome improving intracellular drug delivery [Problem] To provide a drug delivery system which is retained in the blood circulation and improves pharmacological effect of the drug in the target organ and cell. [Means for Resolution] A drug-containing liposome for use in the treatment with a liposome prepared by employing polyethylene glycol cholesteryl ether as a part of the liposome-forming agent and using said liposome-forming agent. It is possible to obtain excellent drug effect by further employing a polyethylene glycol diacylglycerol ester as a part of the liposome-forming agent.
US20110009387 Histone h2ax (hh2ax) biomarker for fti sensitivity The present invention relates e.g., to methods for predicting cellular sensitivity to farnesyl protein transferase inhibitors, such as lonafarnib; manumycin A; FTI-276; L-744832; BMS-214662; tipifarnib; BMS-316810K. The methods involve determining if malignant cells exhibit increased expression. of phosphorylated histone H2Ax following contact of one or more of said cells with said inhibitor.
CN101623260B Cefepime hydrochloride proliposome preparation The invention provides cefepime hydrochloride proliposome which comprises the following components by weight part: 3-20 parts of cefepime hydrochloride, 5-40 parts of dipalmitoyl phosphatidyl glycerol, 1-30 parts of cholesterol and 3-50 parts of proppant which consists of sodium chloride and mannitol with a weight ratio of 1:4. The cefepime hydrochloride proliposome greatly improves the stability, has in-vivo degradation of drug carrier liposome, no toxicity and no immunogenicity and can improve the medical therapeutic index and reduce drug toxicity and side effects. The cefepime hydrochloride proliposome can be prepared by conventional processing equipment and industrially and efficiently produced and has low production cost.
CN101234117B Medical use of a pair of ginseng saponin aglycones and their mixture The invention belongs to a filed of medicine technology, which relates to a novel pair of panaxsapogenol and a medical application of a mixture thereof. The pair of compounds are 20(R)-25-methoxyl-dammarane-3beta, 12beta, 20-triol(25Rmdt for short) and 20(S)-25-me-thoxyl-dammarane-3beta, 12beta, 20-triol(25Smdt for short). The 25Rmdt and 25Smdt and the mixture thereof have the antitumor activities of inhibiting the growth and multiplication of a plurality of tumor cells, inducing the differentiation and withering of tumor cells, inhibiting the generation of tumor angiogenic blood vessels, inhibiting the invasion and transfer of tumors, enhancing the body immunity and reducing the toxic and side effects of chemotherapeutic drugs, which is substantially used for treating malignant tumors, with a total effective dosage of 1-100mg/kg/d.
CN101041625A 1,1,14,14-four(2,6-dimethylphenyl)-2,13-dioxygen substitue-6,9-diammonia substitue -4,11-dihydroxy positive tetradecane compound and uses thereof The invention discloses a new compound and application to inhibit the growth of bacillus tubercle in the medical technical domain, whose chemical name is 1, 1, 14, 14-four (2, 6-dimethyl phenyl)-2, 13-dioxo-6, 9-diammonia-4, 11-dihydroxy n-tetradecane (MIC=6.25 mu g/mL).
WO2008001864A1 C-phenyl 1-thioglucitol compound A C-phenyl 1-thioglucitol compound represented by the formula (I), a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the pharmaceutically acceptable salt. (I) wherein X represents a hydrogen atom or a C1-6 alkyl group; Y represents a C1-6 alkylene group or –O-(CH2)n- (n represents an integer ranging from 1 to 5); and Z represents –CONHRA or –NHCONHRB (provided that, when Z represents –NHCONHRB, n is not 1), where RA represents a C1-6 alkyl group substituted by 1 to 3 groups independently selected from a hydroxyl group and –CONH2; and RB represents a hydrogen atom or a C1-6 alkyl group substituted by 1 to 3 groups independently selected from a hydroxyl group and –CONH2. The compound, the salt or the solvate can inhibit the SGLT1 activity to prevent the absorption of glucose or the like, or can inhibit both the SGLT1 activity and the SGLT2 activity to prevent the absorption of glucose or the like and excrete a urine sugar, and is therefore useful as a prophylactic or therapeutic agent for diabetes.
WO2011073662A1 Combination of a benzoxazinone and a further agent for treating respiratory diseases The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclohexyl-N-(2-(2-(5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethylamino)ethyl)-3-(3-(1-methyl-1H-pyrazol-4- yl)phenethoxy)propanamide or a pharmaceutically acceptable salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a muscarinic antagonist; a p38 inhibitor; a PDE inhibitor; a PPARγ agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease (for example chronic obstructive pulmonary disease (COPD) or asthma).
WO2010086709A1 Proteinase-engineered cancer vaccine induces immune responses to prevent cancer and to systemically kill cancer cells A harmless cancer vaccine is made from cancer cells with extracellular proteins including self-recognition molecular patterns being digested by a proteinase. The cancer vaccine is used to vaccinate an individual to induce immune responses against cancer cells systemically. Cancer cells become harmless when they are digested by TumoraseTM. Some proteinases including trypsin cannot kill cancer cells completely and treated cancer cells need to be further processed in order to be harmless and effective. Cancer cells may be from tissue-cultured human or animal cancer cell lines or cancer patients directly. Cancer vaccine vaccinated individuals produce cancer vaccine specific immune responses against cancer cells. Immune response components may be isolated and used to fight against cancer for a cancer patient with a suppressed immune system. Cancer vaccine specific immune components may include cancer vaccine specific polyclonal antibodies, B-cells, T-cells, natural killer cells, monocytes, macrophages and other lymphocytes.
CN103450361A Carboxymethyl cellulose grafted polylactic acid amphiphilic polymer, as well as preparation method and application thereof The invention discloses a carboxymethyl cellulose grafted polylactic acid amphiphilic polymer, as well as a preparation method and an application thereof. The method comprises the following steps: dissolving carboxymethyl cellulose in an ionic liquid to form a homogeneous solution; adding grafting monomers, namely L-lactide monomers and a catalyst, namely stannous octoate into the homogeneous solution; controlling the temperature at 100 DEG C-130 DEG C, performing magnetic stirring, reacting for 18-24 hours in the presence of nitrogen, stopping the reaction and reducing the temperature of a system to room temperature; pouring the reaction system into ethanol to produce a precipitate, filtering and separating the precipitate, and washing with anhydrous ethanol; performing extraction on an obtained product in acetone, and performing vacuum drying to get the purified carboxymethyl cellulose grafted polylactic acid amphiphilic polymer. A dialysis method is utilized for forming self-assembled nanosphere-like micelles of the carboxymethyl cellulose grafted polylactic acid amphiphilic polymer, the particle size is 30-150nm, the critical micelle concentration is 0.01-0.1g/L and the anti-dilution stability is good.
WO2012106118A2 Method of making ophthalmic devices and components thereof from hydrophobic acrylic (ha) polymers with reduced or eliminated glistenings This invention relates to the fields of polymer chemistry, materials science and ophthalmology. More particularly it relates to optical components and method(s) of preparing same from hydrophobic acrylic (HA) monomer(s) that exhibit reduced or eliminated glistenings when implanted in a patient's eye. The method of this invention uses a mixture of one or more low temperature initiators (LTI) combined with one or more high temperature initiators (HTI), to polymerize one or more HA monomers to produce an optical HA polymer which, when used to manufacture an optical component and implanted as with an intraocular lens (IOL), exhibit reduced glistenings to the patient.
US8076356 Triazolopyridinylsulfanyl derivatives as P38 map kinase inhibitors A compound of formula (I), or a pharmaceutical acceptable salt and/or solvate (including hydrate) thereof; and the use of a compound of formula (I) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airways diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.
CN103393635A Application of Nardoaristolones A in preparing medicines for treating rheumatoid arthritis The invention relates to Nardoaristolones A for treating immune inflammation and the Nardoaristolones can be used for preparing medicines for treating rheumatoid arthritis. Terfenadine and diclofenac sodium are taken as control, and the curative effect of Nardoaristolones A is exact. The use of Nardoaristolones A for preparing medicines for treating rheumatoid arthritis provided by the invention is disclosed for the first time. As the framework type belongs to a brand-new framework type, Nardoaristolones A has remarkable substantive characteristics and obviously has remarkable progress for preventing and treating rheumatoid arthritis.
US20090029988 Hydroxyalkyl Substituted Imidazoquinolines Certain imidazoquinolines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-α biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
CN101940631A Method for preparing pollen itching-dispelling pain-relieving tincture The invention discloses a method for preparing pollen itching-dispelling pain-relieving tincture, which is characterized in that: the tincture is prepared from 45 grams of mongolian snakegourd root, 45 grams of dahurian angelica root, 34 grams of short-pedicel aconite root, 4 grams of borneol, 5 grams of camphor, 20 grams of frankincense, 20 grams of myrrh, 10 milliliters of mint oil, 5 milliliters of eucalyptus oil and 5 milliliters of glycerol. By repeated test and comparison, the method for preparing the pollen itching-dispelling pain-relieving tincture can improve the treatment effect of the medicament.
CA2493282A1 Method and composition for inhibiting cancer cell growth using urease and weakly basic anti-cancer compounds Improvements in methods of treating cancer with weakly basic anti-cancer compounds are provided. In one aspect, the invention provides an improvement in a method of treating cancer cells whose extracellular environment contains 1-8 mM urea, by exposing the cells to a weakly basic anti-cancer compound which is effective in inhibiting the growth of the cells. The improvement includes (a) exposing the cells to a urease enzyme composition and, (b) by step (a), reducing the amount of anti-cancer compound required to produce a given extent of inhibition in the growth of the cells when the cells are exposed to the anti-cancer agent. Methods of potentiating the specific therapeutic activity of a weakly basic anti-cancer compound in the treatment of a given mammalian cancer which is responsive to the compound are provided as are pharmaceutical compositions for use in intravenous administration to a subject are also provided.
US20090054464 Hdac inhibitor Compounds having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is pyrrolidinylene or piperidinylene, Y is pyridylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, and salts thereof are useful as a histone deacetylase inhibitors.
US7186741 Neurotensin active 2,3,diaryl-pyrazolidine derivatives The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have inhibiting activity on enzymes which degrade the neuropeptide neurotensin and can be used for the treatment of affections and diseases caused by disturbances of the neurotensin mediated transmission.
US20060247315 Method of treating intestinal disorders with citrulline The present invention relates to the use of L-citrulline (I) for the preparation of a medicament intended for the treatment of pathologies linked to an intestinal insufficiency.
DE102006011111A1 Formulation for analgesic ear drops contains polyhydric alcohol, especially butan-1,3-diol or glycerol, dimethyl sulfoxide and optionally acid or buffer system and dexpanthenol Formulation for introduction into the ear comprises polyhydric alcohol(s) and dimethyl sulfoxide.
CN101474157B Asiatic acid injectable sustained-release microballoons and preparation method thereof The invention relates to the technical field of pharmaceutical preparation, in particular to an asiatic acid sustained-release microsphere used for injection and a preparation method thereof. A biodegradable chitosan is taken as a carrier, an asiatic acid is taken as principal agent, and the asiatic acid sustained-release microsphere used for injection is obtained by the technology of cross-linked emulsion. Due to the obtained medicament carried microspheres, the surfaces are relatively smooth; the particle diameters range from 20mum to 110mum; and the medicament loading rate of the microspheres ranges from 4.8% to 15.6%. The asiatic acid microsphere has the characteristics that the burst effect is modest (the burst size on the first day is smaller than 15%); the release rate is stable; the sustained release time is long (4-10 weeks); and the asiatic acid microsphere is biodegradable. The implantation and the removal by operation before and after the medicament is used are avoided.
CN103127090A Application of Aphanamixoid A in medicines curing kidney cancer The invention discloses application of Aphanamixoid A in medicines curing kidney cancer and belongs to the medicines new use technical field. An external MTT antineoplastic activity evaluation shows that the Aphanamixoid A further has evident inhibiting effect on growth of human kidney cancer cell strain KC. Therefore, the Aphanamixoid A can be used for preparing kidney cancer resisting medicines, and has good development and application prospect. Due to the fact that use of the Aphanamixoid A in preparation of the medicines curing the kidney cancer is made public for the first time, and the skeleton type is completely novel, the Aphanamixoid A has an unexpectedly high kidney cancer inhibitory activity.
US20110287088 Modulation of olfml-3 mediated angiogenesis The present invention relates to nucleic acids and antibodies against Olfml-3 and Olfml-3 protein function in angiogenesis. Angiogenesis-related conditions, such as cancer or wound healing, can be treated by the composition comprising the Olfml-3 antagonists or agonists, respectively.
US20120108592 Pharmaceutical compositions and methods of use of salicylanilides for treatment of hepatitis viruses A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.
US20120295933 Treatment of copd, gastro-esophageal reflux disease (gerd), food allergies and other gastrointestinal conditions and disorders ameliorated by proper histamine management using a combination of histidine decarboxylase inhibators, lra drugs, anti-h1 and/or anti-h2 drugs The invention provides a method for the treatment of COPD and/or gastrointestinal disease conditions ameliorated by histamine management in a subject, comprising administering to the subject an effective amount of a histidine decarboxylase inhibitor.
CN103751127A Novel telmisartan orally disintegrating tablet and preparation method thereof The invention provides a novel telmisartan orally disintegrating tablet with an improved taste, which contains telmisartan, a taste masking agent and pharmaceutically acceptable excipients. The taste masking agent is selected from polymers which can be swollen in water, and preferably is one selected from hydroxypropyl methylcellulose, sodium alginate, sodium carboxymethylcellulose, methyl cellulose and xanthan gum; and the content of the taste masking agent accounts for 10 to 15 wt% of the tablet. In the orally disintegrating tablet, the content of telmisartan as a main component ranges from 5% to 10%. The orally disintegrating tablet also contains a mixture of pharmaceutically acceptable excipients such as bulking agents, disintegrants, surfactants, binders, lubricants and glidants. The telmisartan orally disintegrating tablet offers an excellent taste.
CN102908314A Silybin proliposomes preparation, and preparation method and application method thereof The invention discloses a silybin proliposomes preparation, and a preparation method and application method thereof, belonging to pharmaceutical technical field. The silybin proliposomes preparation comprises the following materials by weight: 0.8-1% of silybin, 4-17% of phospholipids, 0.22-0.43% of sodium oleate, and the balance of ethyl lactate or 1,2-propylene glycol. The silybin proliposomes preparation effectively applies proliposomes preparation method into silybin extract, to create a new silybin lipid dosage form; utilizes liver targeting characteristic of lipid, to concentrate silybin at liver site after administration, thereby improving silybin curative effect and effectively reducing side effects; and utilizes absorption-promoting effect of lipid, to improve in-vivo bioavailability of silybin compared with silybin material drug, thereby overcoming the defects of existing silybin preparations such as poor absorption and low bioavailability.
CN102631320A Betahistine hydrochloride liposome and preparation method thereof The invention relates to a betahistine hydrochloride liposome and a preparation method of the betahistine hydrochloride liposome. The preparation method comprises the steps of: firstly dissolving lipide ingredients in methylene dichloride, and carrying out reduced-pressure evaporation in water bath until a film is formed; dissolving the film in diethyl ether, and then adding phosphate buffer containing betahistine into the solution; carrying out ultrasonic treatment on the mixed suspension liquid, placing the treated liquid on a rotary evaporator, and carrying out reduced-pressure vaporization until all the organic reagent is evaporated; and finally, obtaining the betahistine hydrochloride liposome. The betahistine hydrochloride is made into liposome, so that the medicine effect is obviously improved, the permeability of blood capillary can be improved, and the dosage of the medicine reaching blood vessels of the brain can be increased; the betahistine hydrochloride liposome is used for improving the treatment effect of Meniere syndrome, reduces the gastrointestinal irritation and the adverse drug reaction, and is beneficial to reducing the side effects such as stomach upset, nausea, dizziness and the like.
US20050026251 Netrin receptor protein for use in identification of modulator for use in treatment and prevention of infection, nervous system, autoimmune, inflammatory, psycological and reproductive disorders The invention is based on the discovery that the INSP017 protein functions as a trans-membrane protein molecule, preferably as a trans-membrane protein molecule of the netrin receptor family.
WO2014096155A1 Glutamate derivatives for topical use as immunomodulatory active ingredient The present invention relates to L-glutamate-derived compounds of general formula (I) in which the R radical is a linear or branched C5 to C2 alkyl group, • - or the benzyl radical, • - or the phenethyl radical, for topical use as a medicament (or as a dermatological active ingredient) intended for the treatment and/or prevention of inflammatory dermatoses.
CN101513528A Compound chemotherapy medicament for treating liver cancer and multi-drug resistance tumor The invention discloses medicinal application of a compound chemotherapy medicament of artemisinins (dihydroartemisinin, artemisinin succinate, artemisinin methyl ether, or artemisinin ethyl ether), glutathione depleting agents (diethyl maleate, N-ethyl-maleimide or buthionine sulfoximine) and antioxidant enzyme inhibitors (mercapto-succinic acid and 3-amino-triazole), wherein the compound chemotherapy medicament can be used as the compound chemotherapy medicament for liver cancer and multi-drug resistance tumor with efficient, quick effect, low toxicity and low cost. Liver cancer and multi-drug resistance tumor patients orally take the medicament or are applied by intravenous injection; the everyday treatment dosage comprises 1 to 100 milligrams per kilogram of the dihydroartemisinin, the artemisinin succinate, the artemisinin methyl ether or the artemisinin ethyl ether, 1 to 80 millimoles per kilogram of the diethyl maleate, the N-ethyl-maleimide or the buthionine sulfoximine, 1 to 50 milligrams per kilogram of the mercapto-succinic acid, and 1 to 50 milligrams per kilogram of the 3-amino-triazole; the medicament can be used once or repeatedly; and after the treatment, the tumor can disappear or the proliferation of the tumor can be controlled, so the patients can live for a long time and work normally.
WO2009028457A1 Therapeutic agent for nonalcoholic steatohepatitis Disclosed is a therapeutic agent for nonalcoholic steatohepatitis (NASH), which can be clinically used for the treatment of a patient suffering from mild or severe non-alcoholic steatohepatitis, which has an excellent pharmacological effect on fatty liver or hepatitis, which is safe and therefore can be ingested over a long period, and which has no adverse side effect. Also disclosed is an agent for improving the liver function in a patient suffering from nonalcoholic fatty liver disease (NAFLD). The therapeutic agent for nonalcoholic steatohepatitis comprises at least one unsaturated fatty acid selected from eicosapentaenoic acid having a high purity of at least 98%, salts thereof and esters thereof. The agent for improving the function of liver tissue comprises the unsaturated fatty acid and can improve liver tissue dysfunctions such as fatty liver and/or hepatitis.
CN101732779A Novel method for lowering breath resistance of bronchial asthma The invention discloses a novel method for lowering the breath resistance of the bronchus, which achieves the aim of treating asthma by the function of suppressing MLCK and still belongs to the first time at home and even abroad. The preparation of an MLCK gene knockout mouse and the research of the contraction function of the MLCK gene knockout mouse confirm the key function of the MLCK in the contraction of the smooth muscle of the air duct so as to confirm that the breath resistance of the bronchus can be obviously lowered under the conditions of physiology and pathology by suppressing the MLCK, thereby making a sufficient preparation for the next artificial synthesis of an MLCK suppressor used for treating the asthma. The invention not only finds the novel method for lowering the breath resistance of the bronchus but also provides a concept for developing other treatment schemes afterwards.
EP1718602A4 Therapeutic and carrier molecules The present invention relates generally to compounds comprising a hydrocarbon chain portion and more particular to compounds comprising chemical derivatizations of the hydrocarbon chain which are useful therapeutic and prophylactic molecules. The present invention further provides compounds where the hydrocarbon chain portion is a carrier molecule for functional groups, moieties or agents. The compounds of the present invention are particularly useful in the treatment and prophylaxis of a range of conditions including cancers, protein kinase c(PKC)- or NFkB-related- or -associated conditions, cardiovascular conditions, pain, inflammatory conditions, vascular or immunological conditions such as diabetes, neurological conditions and infection by a range of viruses or prokaryotic or eukaryotic organisms. The present invention further provides pharmaceutical compositions and methods of medical treatment.
WO2013088445A1 Pyrimidine derivatives for treatment of inflammatory diseases Small pyrimidine derivatives of the formula I useful for treatment of an inflammatory disease or a central nervous system (CNS) injury, particularly for treatment of rheumatoid arthritis, multiple sclerosis, cerebral ischemia or spinal cord injury.
US20120196918 PREVENTING ISLET INFLAMMATION AND DYSFUNCTION AND MAINTAINING PROPER GLUCOSE LEVELS BY CONTROLLING eIF5A AND ITS HYPUSINATION Pancreatic islet dysfunction, in both type 1 and type 2 diabetes results, in part, from cytokine-mediated inflammation leading to iNOS generation and the death of pancreatic islets. The production of pro-inflammatory cytokines involved in the generation of iNOS is facilitated by the availability of the hypusine-containing translational factor eIF5A, necessary for the maturation of antigen-presenting cells. Treatment with agents capable of interfering with the mRNA translating iNOS or with agents that can interfere with the hypusination of eIF5A, prevents the death of islets, lowers blood glucose levels, avoids insulin resistance, and generally avoids the inflammatory response in islets associated with type 1 and type 2 diabetes.
CN102743399A Application of mulberroside to preparation of diuretic medicine The invention belongs to the field of pharmaceutical chemistry, and provides application of mulberroside to preparation of diuretic medicine. The mulberroside has a structure of 3-[2-(4-(beta-D-glucopyranosyl-O-2-hydroxyphenyl)]-(E)-vinyl]-5-hydroxyphenyl-beta-D-glucopyranoside. The invention also provides a diuretic medical composition, which comprises mulberroside with an effective amount and pharmaceutically acceptable carrier. Research by the invention shows that mulberroside has the effect to increase urine amount of rabbits, and has characteristics of mild diuretic effect and persistency.
WO2006104396A1 Pre-complexed copper antagonist compositions Pharmaceutical compositions having a pharmaceutically acceptable copper antagonist compound, for example, copper (II) antagonist(s), complexed to a pharmaceutically acceptable non-copper metal ion, articles and kits and delivery devices containing such compositions, tablets and capsules and formulations containing such compositions, and methods of use for treatment of subjects, including humans, who have or are at risk for various diseases, disorders, and conditions.
CN102924450A 6-(5-pyridyl)-1,2,4-triazolopyridine compound, and preparation method and application thereof The invention discloses a 6-(5-pyridyl)-1,2,4-triazolopyridine compound, and a preparation method and application thereof. The medical compound is novel in structure, and the synthesis method is easy to realize. The compound has obvious antineoplastic activity and can be used for antineoplastic preparation. Determination of antineoplastic activity on cell proliferation indicates that the synthesized compound has obvious inhibiting action on the proliferation of human colon cancer cells HCT116 and human brain glioma cells U87.
CN102627613A 2-[(4,6-dimethyl pyrimidine-2-)oxyl]-3-cyano-3,3-dibenzyl propionic acid optical isomer, its preparation method and medical application The invention relates to an optically pure compound, a preparation method and its medical application, specifically to a 2-[(4, 6-dimethyl pyrimidine-2-)oxyl]-3-cyano-3,3-dibenzyl propionic acid optical isomer, its preparation method and a medical application.
US7771711 Sphingolipids' polyalkylamines conjugates The present invention concerns novel sphingolipid-polyalkylamines conjugates, a process for their preparation and pharmaceutical compositions comprising the same. In particular, the present invention concerns ceramide based polyalkylamine conjugates and its use as a capturing agent. A preferred ceramide polyalkylamine conjugate is a ceramide-spermine conjugate, more preferably, N-palmitoyl D-erythro sphingosyl-1-carbamoyl spermine.
CN102552283A Transdermal absorption drug for skin prepared from hydrocortisone butyrate containing adjuvant and water containing adjuvant The invention relates to a transdermal absorption drug for skin prepared from hydrocortisone butyrate containing adjuvant and water containing adjuvant. The transdermal absorption drug is prepared from single-packaged hydrocortisone butyrate and single-packaged water, wherein the hydrocortisone butyrate contains one or several kinds of solid pharmaceutical adjuvant and is difficult to dissolve in water, and the D90 grain size of the hydrocortisone butyrate is 0.1-10mum; and the water contains one or several kinds of water-soluble pharmaceutical adjuvant.
CN101107233A 1H-imidiazole derivatives as cannabinoid CB2 receptor modulators The invention relates to a group of 1 H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1 H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.
US20120093752 Use of Monoamine Oxidase Inhibitors to Improve Epithelial Biology The invention provides a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analogue, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided.
US20140142077 Androgen pharmaceutical composition and method for treating depression The present invention relates to methods, kits, combinations, and compositions for treating, preventing or reducing the risk of developing a depressive disorder, or the symptoms associated with, or related to a depressive disorder in a subject in need thereof. The present invention also relates to a method of administering a steroid in the testosterone synthetic pathway, for example testosterone, to a subject in need thereof. In addition, the methods, kits, combinations and compositions may be used in conjunction with other pharmaceutical agents including agents effective at treating, preventing, or reducing the risk of developing a depressive disorder in a subject.
US20070044795 Method and apparatus for dispensing inhalator medicament An apparatus and method for delivering a plurality of medication includes providing first and second medicament on a medicament pack in separate containers for preventing either medicament from interfering with the stability of the other. In accordance with the method, the medicaments are preferably delivered in a single inhalation.
WO2006035283A1 Oxazolidinone derivatives as antimicrobials The present invention relates to substituted phenyl oxazolidinones and processes for preparing thereof. This invention also relates to pharmaceutical compositions comprising compounds of the present invention. Such compounds can be useful antimicrobial agents that can be particularly effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria (e.g., multiple-resistant staphylococci, streptococci and enterococci), anaerobic organisms (e.g., Bacterioides spp. and Clostridia spp. species), and acid-fast organisms (e.g., Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp).Formula (I).
CN101961349A Sea cucumber reinforced agglutinin and method thereof for preventing sea cucumber infective diseases The invention relates to a reinforcing agent for a comprehensive culture method for sea cucumber and a method thereof for preventing and treating sea cucumber diseases with infectivity in sea cucumber culture, in particular to sea cucumber reinforced agglutinin and a method thereof for preventing sea cucumber infective diseases. The formula of the agglutinin comprises ammonium chloride, sodium hydrogen carbonate, potassium acid phosphate, sodium acetate, magnesium sulfate heptahydrate, sodium chloride, distilled water and the like. Endogenous agglutinin in the sea cucumber body is used as immune molecules of the sea cucumber and can generate immune response aiming at external bacteria or pathogenic bacteria; when the immune function of the sea cucumber is reduced, the agglutinin of the sea cucumber cannot be totally combined with carbohydrate-binding proteins on the surfaces of the bacteria, and then the sea cucumber suffers from various diseases; and if exogenous agglutinin with a plurality of carbohydrate identification areas is added at the moment, the agglutinin is specifically combined with carbohydrate links and carbohydrate-binding proteins on the surfaces of the bacteria and can specifically disturb the combination of pathogens and hosts.
CN102872037A Application of Gypensapogenin B in medicaments against aseptic inflammation The invention relates to an application of Gypensapogenin B in medicaments against inflammation, wherein the inflammation is aseptic inflammation, and Gypensapogenin B has good anti-inflammation and antiphlogistic effects. The application of Gypensapogenin B in preparing medicaments against inflammation, involved in the invention, is disclosed for the first time. As the skeleton is brand new, andthe strong activity of Gypensapogenin B on inhibiting inflammation is unexpectedly strong, the possibility that any enlightenments are given by other compounds does not exist. Gypensapogenin B has prominent substantive features and has notable progress when being used for the anti-inflammation application.
US20120101132 New Substituted Oxindole Derivative The present invention relates to a new compound of formula (I) 6-(5-cyano-2-hydroxy-1H-indol-3-yl)pyridine-3-carboxylic acid or a pharmaceutically acceptable salt thereof, in an essentially pure and isolated form, pharmaceutical formulations containing said compounds, to the use of said active compounds in therapy, and methods of prevention and/or treatment of conditions associated with glycogen synthase kinase-3 related disorders, comprising administering to a mammal, including human in need of such prevention and/or treatment, a therapeutically effective amount of said compound, as well as a process for preparing said compound.
US20120028929 Tetracycline stabilizing formulations An aqueous solution comprising a chelating agent at a concentration of about 0.1-0.5%, and an antioxidant agent at a concentration of about 0.1-0.5%, wherein the pH of the solution is between about 4.5 and about 7.5 is disclosed. The aqueous solution may comprise a tetracycline composition wherein the tetracycline is formulated in the aqueous solution. A method for reducing the rate and/or overall extent of degradation of a tetracycline in aqueous solution, comprising admixing in a tetracycline containing solution a chelating agent at a concentration of about 0.1-0.5% and an antioxidant at a concentration of about 0.1-0.5% and, as necessary, adjusting the pH of the solution so that it is between about 4.5 and about 7.5 is also disclosed. Tetracycline compositions of the invention may be used to treat inflammatory and/or tissue degeneration conditions.
US20130072550 PKC ACTIVATION AS A MEANS FOR ENHANCING sAPPalpha SECRETION AND IMROVING COGNITION USING BRYOSTATIN TYPE COMPOUNDS The present disclosure relates to methods of administering compounds for treating conditions associated with amyloid processing such as Alzheimer's Disease. Methods are disclosed comprising the step of administering a macrocyclic lactone, a benzolactam, a pyrrolidinone or a combination thereof to a subject in need in an amount effective to decrease soluble Aβ-40 or Aβ-42, or to lower total amyloid precursor protein (“APP”). Methods are also disclosed further comprising the step of identifying a subject with increased soluble Aβ-40 or Aβ-42 levels, or elevated APP levels compared to a control population.
CN103405425A Application of Chukrasone B in medicine for treating lung cancer The invention discloses application of Chukrasone B in preparation of a medicine for treating lung cancer, and belongs to the technical field of new application of medicines. The compound shows high lung cancer inhibition activity and can be used for preparing the medicine for treating lung cancer. The in-vitro MTT (3-4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) antitumor activity evaluation shows that Chukrasone B has remarkable inhibition effects on in vitro cultured non-small cell lung cancer cell A549, large cell lung cancer cell NCI-H460, lung squamous cancer cell HTB-8 and human lung squamous cell carcinoma cell QG-5, but has little inhibition effect on human normal hepatocyte LO2 and peripheral blood lymphocyte, so that Chukrasone B has the characteristic of obvious selectivitya. The application of Chukrasone B in the preparation of the medicine for treating lung cancer is disclosed for the first time; the framework type of Chukrasone B is brand new; Chukrasone B brings unexpected inhibition activity for lung cancer cells.
WO2012088388A2 Treating multiple myeloma This document relates to methods and materials for treating multiple myeloma. For example, methods and materials for using albumin-bound paclitaxel composition (e.g., Abraxane®, a paclitaxel albumin-stabilized nanoparticle formulation) to treat multiple myeloma are provided.
US20110152379 Composition for control of aging and/or extension of life, containing dapsone as active ingredient The present invention relates to a composition for controlling aging and/or extending lifespan. More specifically, the present invention relates to a composition containing dapsone as an effective component for controlling aging and/or extending lifespan, in which when applying the composition according to the present invention to an object, the effect of controlling aging or extending lifespan is excellent. Specifically, the treatment of dapsone (DDS) increases the lifespan of C. elegans not depending upon daf-16 and delays aging process, and reduces the activity of cytoplasmic dual oxidase 1 (Duox1) and mitochondria complex V protein. In addition, dapsone can maintain the low oxygen uptake rate in C. elegans thereby reducing ROS formation. In addition, ROS production by paraquat that is an inducing material of oxidative stress is reduced by treating dapsone and the sensitivity of paraquat is reduced. Moreover, it can be known that pyruvate kinase is a target material of dapsone through the structural prediction, molecular and biochemical analysis. In addition, there is an effect that the recovery of mitochondria function that is reduced and the decrease of NOX expression in a cell are obtained by dapsone in the human diploid fibroblast. From the comprehensive results, it can be known that dapsone has an excellent effect for extending lifespan in a cell level and object level.
WO2005113014A1 siRNA TO VP-1 OF JC VIRUS AND MEDICINAL COMPOSITION CONTAINING THE SAME [PROBLEMS] To provide a medicinal composition for treating JC virus infection such as progressive multifocal leukoencephalopathy (PML) by inhibiting the expression of VP-1 and inhibiting the proliferation of JC virus, a polynucleotide therefor and utilization of the same. [MEANS FOR SOLVING PROBLEMS] It is intended to provide a medicinal composition for treating JC virus-infected cells by the RNAi method with the use of a short interfering RNA (siRNA) to a gene encoding VP-1 of JC virus and a polynucleotide which is the active ingredient therefor. Namely, a medicinal composition for treating JC virus infection comprising a short interfering RNA (siRNA) to a gene encoding VP-1 of JC virus or a gene capable of forming this siRNA and a pharmaceutically acceptable carrier; a polynucleotide therefor; and utilization for producing the same.
CN101744762B Preparation method of butenafine hydrochloride liniment The invention discloses a preparation method of butenafine hydrochloride liniment. Firstly butenafine hydrochloride hydroxypropyl-beta-cyclodextrin clathrate compound is prepared and then the clathrate compound is dissolved to prepare a liniment. In the process of preparing the clathrate compound, the weight ratio of the butenafine hydrochloride and the hydroxypropyl-beta-cyclodextrin, the constant temperature blending time, the blending speed and the temperature are optimally selected. The inclusion of the butenafine hydrochloride by the hydroxypropyl-beta-cyclodextrin enhances the solubility of the butenafine hydrochloride, thereby solving the problem of poor water solubility of the butenafine hydrochloride. Meanwhile, the preparation method significantly reduces the consumption of ethanol, thus reducing the irritation of the liniment to the skin of the user.
CN101953807A Mycophenolate mofetil lyophilized powder injection for injection and preparation method thereof The invention provides a mycophenolate mofetil lyophilized powder injection for injection. The injection is prepared from mycophenolate mofetil serving as an active ingredient and polyethylene glycol-12-hydroxy stearate serving as a solubilizing agent in a weight ratio of 250-1,250:100-500. The invention also provides a method for preparing the mycophenolate mofetil lyophilized powder injection for injection. The mycophenolate mofetil lyophilized powder injection for injection has the advantages of simple and reasonable prescription, stable quality, convenient use, capabilities of preventing adverse reactions such as nausea, vomit, diarrhea and the like caused by oral preparations and the like and preventing toxic or side effects such as drop of blood pressure, hemolysis and the like caused by solubilizing agents such as Twain 80 and the like, high safety and good application prospect.
CN102600129A Application of andrographolide C15 substitution derivative in manufacturing anti-hepatitis drug The invention discloses the application of an andrographolide C15 substitution derivative in manufacturing an anti-hepatitis drug, which belongs to the technical field of pharmaceutical chemistry. According to the invention, MDBK (mardin-darby bovine kidney cells) and BVDV (bovine viral diarrhea virus) are utilized to study the inhibitory action of the compound on cytopathic effect caused by the virus through an external screening model. Through the screening of a large number of andrographolide derivatives, the compound with a structure of general formula 1 is found to significantly inhibit MDBK cytopathic effect caused by the BVDV; the andrographolide C15 substitution derivative has high efficiency and low toxicity, thereby being used for manufacturing medicaments for treating and preventing hepatitis and having good prospect in development and application. The general formula 1 is as follows.
WO2014044721A1 Novel crystalline form of vortioxetine hydrobromide The present invention is directed to a crystalline compound comprising a hydrobromide acid (HBr) salt of a compound of formula (I) (1-{2-[(2,4-dimethylphenyl)sulfanyl]phenyl}piperazine, INN: vortioxetine), having an XRPD pattern with characteristic peaks (expressed in 2θ ± 0,2° 2θ (CuKα radiation)) at 5.5°, 14.8°, 16.7° and 20.0° and processes for obtaining the same.
US20110306676 Method and Medicament for Pain Management The present invention relates to a method and an apparatus for treating pain in a patient, such as a veterinary patient. The method comprises the step of administering an inhalation anaesthetic at sub-anaesthetic levels to the patient during an anaesthesia of the patient. A suitable agent may be methoxyflurane.
EP2259677A2 Systemic purine administration:modulating axonal outgrowth of central nervous system neurons Methods for modulating the axonal outgrowth of central nervous system neurons are provided by means of internalized purine administration such as by intravenous, intraarterial, subcutaneous, intramuscular, intraperitoneal, and intrapleural administration. The methods are noted for stimulating the axonal outgrowth of central nervous system neurons following an injury (e.g., stroke, traumatic brain injury, cerebral aneurism, spinal cord injury and the like).
US7105572 Cardiovascular disorders An emulsion composition containing a compound represented by the formula: wherein R, R0, Ar and n are as defined in the specification or a salt thereof or a prodrug thereof, wherein the composition is adjusted to have a pH of not more than about 6, shows improved stability of the compound, a salt thereof or a prodrug thereof, and realizes expression of superior efficacy.
CN101983678A Pharmaceutical composition for accelerating wound healing and preparation method thereof The invention discloses a pharmaceutical composition for accelerating wound healing and preparation method thereof. The pharmaceutical composition consists of radix aconite, radix aconiti kusnezoffi, unprocessed rhizoma arisaematis, raw pinellia ternate, Chinese honey locust and unprocessed frankincense. Treatment with the above pharmaceutical composition, which is suitable for emergency uses, has the advantages of easy operation, convenient carrying, fast homeostasis and analgesia, low expense and rapid healing.
CN102718696A Preparation method and anti-AIDS purpose of Baculiferin L and analog thereof The invention discloses a preparation methodof Baculiferin L and analogs (see the following formula) thereof. I is prepared under protection of inert gas by a substituted phenylacetaldehyde and an amino compound or ammonia gas; II is obtained through a reaction between I and 2-bromo-2-(3,4-dimethoxy benzyl) acetic acid trichloroethyl alcohol ester under an condition of acidic alumina; III is obtained through a reaction among II and zinc dust and an ammonium acetate solution; IV is obtained through a reaction among III and potassium acetate and acetic anhydride; V is obtained through a reaction in an organic solvent between IV and a sodium hydroxide solution; Baculiferin L and analogs thereof are obtained under protection of inert gas by V and boron tribromide in the presence of organic solvent. The method is characterized by fewer steps, simple process, and high yield; and precious metal catalysts are not needed. The method saves energy, reduces emission, and has high efficiency. The invention also discloses the anti-AIDS related applications of Baculiferin L and analogs thereof aiming at AIDS key targets like Vif, APOBEC3G, pg41, and the like.
US7291641 Derivatives of heterocycles with 5 members, their preparation and their use as medicaments Thiaxozle, oxazole, imidazole, isoxazole and isoxazoline compounds of the formula wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is selected from the various optionally substituted aromatic radicals defined in the specification, B is hydrogen, alkyl or phenyl, R1 and R2 are independently hydrogen, alkyl or cycloalkyl or R1 and R2 taken together with the carbon atom which carries them, form a carbocycle with 3 to 7 members and Ω is —NH46R47 or —OR48, R46 and R47 are independently hydrogen, alkyl, cycloalkyl or —(CH2)kCOOR51, R51 is alkyl or haloalkyl and R48 is hydrogen or alkyl having advantageous pharmacological properties which allow their use in therapeutics, for treating neurodegenerative disorders or pain.
EP1867647A1 Substituted aminopyrazolopyridines and salts thereof, their preparations and pharmaceutical compositions comprising them. The invention relates to substituted aminopyrazolopyridines according to the general formula (I) : in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted aminopyrazolopyridines, to methods of preparing said substituted aminopyrazolopyridines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
EP1513858A2 Process for the preparation of heterocyclyl substituted adenosine derivatives The present invention relates to an improved process for the preparation of heterocyclyl substituted adenosine derivatives. More particularly the invention is concerned with preparation of particular physical forms of (2S, 3S, 4R, 5R)-2-(5 tert-butyl-[1,3,4]oxadiazol-2-yl)-5-[6-(4-chloro-2-fluoro-phenylamino)-9H-purin-9-yl]-tetrahydro-furan-3,4-diol.
EP1507760A1 Cyanoguanidine prodrugs Pyridyl cyanoguanidine compounds of the general formula I wherein A, X1, X2, X3, Y1, Y2, Y3, R1, R2, R5, R6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseases such as cancers.
WO2010103472A1 Cosmetic use of an extract of wolfberry for treating scalp disorders The present invention relates to the use of an effective amount of an extract of wolfberry, and in particular of lacto-wolfberry, for preventing and/or treating dandruff disorders of the scalp.
EP2305653A1 Therapeutic agent for chronic renal failure The present invention aims to provide a therapeutic agent for chronic renal failure, comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof. That is, the present invention provides provision of a drug comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof, which drug is useful not only for amelioration of renal function, but also for amelioration of anemia, activation of SOD and excretion of uremic substances.
US20100256233 Systems, methods and compositions for reduction of injury from radiation exposure Some embodiments of the invention comprise systems, methods and/or compositions for the systemic use of histone deacetylase inhibitors (“HDACi”) to protect against or alleviate the effects of radiation exposure, whether due to hostile actions, such as terrorist activity; through therapeutic radiation exposure; or through other methods of intentional or unintentional exposure to radiation, including but not limited to, total body irradiation.
US20070071794 Drugs for treating diabetes The present invention provides an agent for recovering insulin secretion function which contains at least one of the amino acids selected from the group consisting of aspartic acid, cystine, serine, asparagine, isoleucine, histidine, hydroxyproline, glutamic acid, valine and salts thereof as an active ingredient; a functional food which contains the agent for recovering insulin secretion function; and a composition for treating diabetes which contains the amino acid(s) and a second diabetic drug as active ingredients. This agent for recovering insulin secretion function can be used as an oral therapeutic agent or functional food that is useful for treating, improving or preventing insulin secretion defects in Type II diabetes, borderline diabetes and other diseases, and side effects caused by administration of drugs.
US20120101073 Novel Method For Treating Breathing Disorders or Diseases The present invention includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation comprising (+)-doxapram or a salt thereof, and a pharmaceutically acceptable carrier, wherein the formulation is essentially free of (−)-doxapram or a salt thereof.
EP1326639B1 Adjuvant composition comprising an immunostimulatory oligonucleotide and a tocol The present invention relates to novel adjuvant compositions for use in vaccines. In particular, the adjuvant compositions of the present invention comprise a combination of an immunostimulatory oligonucleotide and a tocol. Also provided by the present invention are vaccines comprising the adjuvant compositions of the present invention and at least one antigen. Further provided are methods of manufacture of the adjuvant compositions and vaccines of the present invention and their us as medicaments. Additionally, the present invention provides methods of treating an individual susceptible to or suffering from a disease by the parenteral or mucosal administration of the vaccines of the present invention.
EP2057284A1 Compositions and methods for the modulation of jnk proteins The invention provides compositions and methods for the treatment and diagnosis of diseases or disorders amenable to treatment through modulation of expression of a gene encoding a Jun N-terminal kinase 1 (JNK l protein.
CN102020537A Protein tyrosine phosphatase 1B (PTP1B) inhibitor, and synthesis and application thereof The invention relates to a chemical total synthesis method for a novel protein tyrosine phosphatase 1B (PTP1B) inhibitor and the application of the PTP1B inhibitor to medicaments for treating type 2 diabetes mellitus. The PTB1B inhibitor has a chemical structural formula, wherein groups connected with carbon atoms at 2, 2', 3, 3' and 6 positions are bromine atoms; and carbon atoms at 4, 4', 5 and 5' positions are connected with hydroxide radicals. The chemical name of the PTP1B inhibitor is (2',3'-dibromo-4',5'-dihydroxy-phenyl)-(2,3,6-tribromo-4,5-dihydroxy-phenyl)-methane. The compound inhibits the activity of protein tyrosine phosphatase 1B to enhance the sensitivity of an insulin receptor, and has a good therapeutic effect on the insulin-resistant type 2 diabetes mellitus.
WO2008080170A1 Mixed drug aerosol compositiions The present invention pertains to aerosols which comprise a first compound which is physiologically active and a second compound which is different from the first compound. Such aerosols may be produced 'on demand' and can be used to control drug release, to improve vaporizability, or to reduce, modify or eliminate undesirable taste associated with a drug aerosol. The present invention also pertains to methods for producing such aerosols.
US20080274149 Encapsulation and Controlled Release of Biologically Active Ingredients with Enzymatically Degradable Microparticulate, Hyperbranched Polymers The invention provides encapsulated, microparticulate active ingredient formulations for the controlled release of active ingredients on skin and skin appendages consisting of encapsulation material as casing and at least one enclosed biologically active ingredient as core, which is characterized in that enzymatically degradable organic hyperbranched polymers containing ester groups are used as encapsulation material.
WO2009020140A1 Adamantylurea derivative Disclosed is a compound represented by the formula (1) below, which is useful as an agent for prevention or/and treatment of diabetes and the like, or a pharmaceutically acceptable salt of such a compound. (In the formula, A represents a hydroxy group, CONR1R2 or the like, wherein R1 and R2 independently represent a hydrogen atom or the like; and ring B represents a group represented by the following formula (G1) or the like.) (In the formula (G1), a represents a number of 0-5; b represents a number of 1-4; X1 represents a single bond, -O-, -CO- or the like; and X2 represents an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted cycloalkyl group or the like.)
US20120252767 Methods of Hormonal Treatment Utilizing Ascending-Dose Extended Cycle Regimens The present invention provides ascending-dose extended cycle regimens in which a female is administered an estrogen and a progestin for a period of greater than 30 or 31 consecutive days, optionally followed by a hormone-free period or by a period of administration of estrogen. The disclosed regimens can be administered to a female to provide contraceptive and non-contraceptive benefits.
US7754701 toothpastes, mouthwashes, chewing gums, tableted candy, for inhibiting induction of dental caries The present invention relates to a difructose anhydride (DFA)-containing composition and use thereof. DFA is a cyclic disaccharide in which the reducing termini of two fructose molecules bind each other to hydroxyl groups at the other nonreducing termini. According to the present invention, it has been revealed that DFA is effective in accelerating the absorption of magnesium, zinc or copper, accelerating bone formation, accelerating diuretic action, and improving bowel movement and is useful in inhibiting dental caries. A composition of the present invention can be used as a composition for a medicinal product and a food or drink product (including feed for animal use). Examples of a medicinal product and a food or drink product for human or animal use include formulated powder milk, parenteral nutrients, health food and drink products, and additives for feed and are not particularly limited as long as they are ultimately in an orally administrable form.
US7030087 A water-soluble polypeptide having hydrophobic side chains, for use as bactericides treating infections, detoxification of endotoxin, cell antiproliferative agents, antagonist of tumor necrosis factor This invention relates to the chemical design and production of peptides, peptide structure and three dimensional conformation was assessed using NMR, circular dichroisin and pulsed field gradient NMR. In addition, this invention relates to peptides produced by these methods and to methods for using the peptides.
CN101279082A Analgesic medicament for curing burn, scald and injure caused by poisonous honey The invention relates to a medicine for curing burns and in particular discloses an analgesic medicine for burn, scald and sting by toxic bee. The preparation method of the medicine is that: a certain proportion of radix rehmanniae or prepared radix rehmanniae is sliced and baked, ground into powder and added to a container filled with Dieda Wanhua oil for evenly mixing and then the medicine is prepared. The medicine not only has simple preparation process, low price and good analgesic effect, but also can alleviate pains of sufferers within a short time; the medicine not only has remarkable curative effect on burn, scald, but also has special curative effect on sting by toxic bee.
WO2010086878A3 Thyroid receptor modulators The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta. Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.
US20100267798 Pharmaceutical formulations and use thereof in the prevention of stroke, diabetes and/or congestive heart failure The present invention relates to use of an inhibitor of the renin-angiotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).
CN102863501A Spirostanol glycoside-type compound, and application and preparation method thereof The invention discloses a spirostanol glycoside-type compound, and application and a preparation method thereof. The invention provides the application of the spirostanol glycoside-type compound to the preparation of anti-hypoxic medicines or food. The spirostanol glycoside-type compound has the following general structural formula. The method for preparing the spirostanol glycoside-type compound comprises the following steps of: crushing dried selaginella uncinata spring, and performing reflux extraction on the crushed selaginella uncinata spring by adding a solvent or water; removing insoluble substances by filtration or centrifugation, and drying under reduced pressure to obtain initial extract; dispersing the initial extract into isometric water, and performing extraction by adding petroleum ether, chloroform, ethyl acetate and normal butyl alcohol in sequence; and drying the liquid extract of normal butyl alcohol under reduced pressure to obtain extract of normal butyl alcohol; and separating and purifying the extract of normal butyl alcohol by the chromatography to obtain the spirostanol glycoside-type compound.
WO2012163264A1 Saucernetin structurally simplified substance and preparation method therefor and pharmaceutical composition and use thereof Disclosed a saucernetin structurally simplified substance and the preparation method and pharmaceutical composition and use thereof. In particular, it relates to a compound of general formula (I) shown as formula (I) or an isomer thereof and a salt thereof, and the preparation method for such compounds. A novel pharmaceutical composition contains an effective amount of compound of formula I and a pharmacodynamically acceptable vector. The present invention also discloses the use of such compounds in preparing drugs for preventing and/or treating tumours. The tumours include neural glioblastoma, melanoma, gastric cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermoid carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer, and colon cancer and rectal adenocarcinoma.
US20110009395 Bace inhibitors The present invention provides BACE inhibitors of Formula I: methods for their use, intermediates, and methods for their preparation.
WO2008125627A1 Pyridazine-, pyridine- and pyrane-derivatives as gpbar1 agonisis A compound of formula (I) wherein the substituents have various meanings, optionally in salt and/or solvate form, and their use as pharmaceuticals.
US20080300278 central nervous system disorders; respiratory system disorders; sexual or reproductive disorders; gastrointestinal disorders; eating disorders; antidiabetic agents; anticancer agents; cardiovascular disorders The present invention relates to prodrugs of pyrazoline compounds of formula I, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
US20080194531 Methods for Treating Visual Disorders The present invention provides methods for treating visual disorders. Exemplary visual disorders include macular degeneration, retinitis pigmentosa, glaucoma, and/or retinal degeneration.
US20100048619 Cold Menthol Receptor Antagonists Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein A, L, R1, R2, R4 and R5 are defined herein.
EP1689714A2 Therapeutic use of pyridinium compounds to modulate naadp activity The present invention relates to the use of a compound of formula (I); wherein: R1 comprises a carbonyl group and R2 is a hydrocarbyl group; optionally wherein said ring is further substituted; or a pharmaceutically acceptable salt thereof; in the manufacture of a medicament for use in one or more of: modulating the release of intracellular calcium from a store controlled by nicotinic acid adenine dinucleotide phosphate; modulating calcium spikes in mammalian cells; treating diseases in one or more of brain, heart, pancreatic cells (e.g. pancreatic acinar and pancreatic beta cells), immune cells, T-cells, haemopoietic cells including phagocytes; treating diseases in one or more of brain, heart, pancreatic cells (e.g. pancreatic acinar and pancreatic beta cells), immune cells, T-cells, haemopoietic cells including phagocytes by modulating the release of intracellular calcium from a store controlled by nicotinic acid adenine dinucleotide phosphate; treating diseases in one or more of brain, heart, and T-cells by modulating calcium spikes in mammalian cells.
CN103159737A Esomeprazole sodium compound and medicine composition The invention belongs to the field of pharmaceutical chemistry, and particularly relates to an esomeprazole sodium compound and a medicine composition. The medicine composition is an injection or an oral preparation. The structural formula of the esomeprazole sodium compound is shown in the specification; and an X-ray powder diffraction spectrogram of the esomeprazole sodium compound, which is obtained through Cu-K alpha ray measurement, is shown in figure 1. The esomeprazole sodium compound provided by the invention has good stability and a strong antibacterial effect on helicobacter pylori; and the esomeprazole sodium freeze-dried powder injection prepared from the esomeprazole sodium compound provided by the invention for injection has good stability, and after the esomeprazole sodium freeze-dried powder injection is combined with 0.9% sodium chloride injection, the insoluble particles of the esomeprazole sodium freeze-dried powder injection changes less within 4 hours. The enteric preparation of the esomeprazole sodium compound has no obvious change and has tolerance to acidity of higher than 93% after being placed for 10 days under the conditions of illumination, high temperature and high humidity; and after being placed at a room temperature for three years, the enteric preparation has no obvious change and has the tolerance to acidity of higher than 95%.
CN103284981A Application of dankasterone A in preparation of antiviral drug The invention discloses a new application of a compound dankasterone A in preparation of an antiviral drug and provides a new application of dankasterone.
US7265125 4-Heteroaminoquinazoline derivatives,.e.g., 2-methyl-4-piperidin-1-yl-7-pyridin-3-yl-quinazoline; prophylaxis or treatment of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity. Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
US7078526 Crystal structured fungicides selected from itraconazole, posaconazole or saperconazole used for prevention or prophylaxis of fungi, yeasts and dermatophyte infections The invention provides novel soluble conazole crystalline forms (e.g. itraconazole, posaconazole and saperconazole) that include salts, co-crystals and related solvates useful as pharmaceuticals. The invention also provides pharmaceutical compositions comprising, and processes for making, these conazole crystalline forms. Methods of using such compositions for the treatment or prevention of systemic and local fungal, yeast, and dermatophyte infections are also provided.
WO2013092481A1 2',4'-difluoro-2'-methyl substituted nucleoside derivatives as inhibitors of hcv rna replication The present disclosure relates to compounds of Formula (I): Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of using the compounds of Formula (I) and/or compositions comprising the compounds of Formula (I) for the treatment of HCV.
US7550496 Hypoxia-activated prodrugs of alkylating agents such as of cyclophosphamide, ifosfamide, melphalan, chlorambucil, thiotepa; protected with 2-nitroimidazolyl group; targeted cancer cells more effectively, side effect reduction Hypoxia-activated prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
US20120202848 Therapy of autoimmune colitis using a tip60 inhibitor This invention is in the fields of immunology and autoimmunity. More particularly it concerns methods of treating patients with compounds which are useful agents for inhibiting the functions of TIP60 in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases.
CN103285397A External compound medicine for treating acne The invention relates to an external compound medicine for treating acne. The external compound medicine is characterized in that a substrate carrier of the external compound medicine contains the following active ingredients, such as non-steroidal anti-inflammatory agents, cimetidine and antibacterial. The external compound medicine has the advantages that the three active ingredients simultaneously act on a plurality of links (anti-inflammation, antibiosis and reduction of sebum secretion) in the acne pathological process. Thus, the curative effect on the acne, especially inflammatory acne is improved; the external compound medicine is high in safety, and free of thrill and anaphylaxis; the contained active ingredients are cheap and available; and the finished medicament is certain to be accepted by wide patients with acnes.
CN102008546A External medical cream for pain and itching relieving and detumescence The invention relates to an external medical cream for pain and itching relieving and detumescence, with extremely-strong sterilizing power. The technical scheme is that the external medical cream for pain and itching relieving and detumescence comprises an auxiliary material of creams and is characterized by further comprising menthol crystal, zinc oxide and double key quaternary ammonium salt.
US20110280882 Leukolectins and uses thereof The present invention relates to a polypeptide, described as a lectin, its encoding nucleic acid sequence and antibodies to the polypeptide and their use in various medical applications, particularly for treating or preventing an autoimmune disorder, an inflammatory disorder or damaged skin in an animal.
US20100190776 Thiazoline and Oxazoline Derivatives and Their Methods of Use The invention relates to a series of thiazoline and oxazoline derivatives, compositions thereof, and methods of treating conditions and disorders using such compounds.
CN103169699A Application of letrozole (LE) in preparation of drug used for causing adult cattle to excessively ovulate The invention provides an application of letrozole (LE) in preparation of a drug used for causing an adult cattle to excessively ovulate. According to the invention, LE is added in the traditional adult cattle superovulation scheme, and follicular development is promoted by utilizing influence of letrozole on internal secretion and paracrine and an ovary follicle collecting effect, so that quantity of available ovocyte is increased; besides, a half-life period of letrozole is shorter, metabolism velocity is high, no side effect is produced, and letrozole can serve as a livestock superovulation auxiliary drug to be popularized and applied in animal husbandry production.
US20120029035 Compositions and methods for extended therapy with aminopyridines Disclosed herein are methods and compositions related to use of aminopyridines, such as 4-aminopyridine, for use in a therapeutically effective manner for patients with a demyelinating condition, such as multiple sclerosis.
US20060034798 Water-in-oil emulsions with ethylene oxide groups, compositions, and methods Water-in-oil emulsions, compositions, and methods that include a vinyl polymer that includes ethylene oxide-containing side chains and alkyl-Y-containing side chains, wherein Y is O or NR, wherein R is H or CH3, and wherein the alkyl group of the alkyl-Y-containing side chain has at least 4 carbon atoms on average in a cyclic, branched-, or straight-chain configuration and optionally including one or more heteroatoms.
US20080057083 Protecting an animal against a pathogen by administering protective agent which is able to stimulate the animal's immune system to produce a response which is protective against the pathogen, and an immunostimulant comprising a polycationic carbohydrate or derivative thereof; non-parenteral immunization A polycationic carbohydrate such as chitosan, or a pharmaceutically acceptable derivative thereof, are used as immunostimulants. Vaccine compositions containing these polycationic carbohydrates, in particular in particles such as microparticles or liposomes are also described and claimed. Methods of treatment and the use of the polycationic carbohydrates as immunostimulants in the production of vaccines are further aspects described and claimed.
WO2013167906A1 Treatment of respiratory depression Tricyclic dibenzothiazepine compounds for use in the treatment of respiratory depression.
US20060281777 Process for preparing crystalline form I of cabergoline A process for producing crystalline form I of cabergoline, which process comprises the preparation of Form V using heptane as precipitation solvent, and its exclusive conversion into crystalline Form I of cabergoline. The present crystallization process from toluene-heptane solvent system for form V involves “reverse addition” of toluene-cabergoline concentrate to cold heptane.
WO2011076687A1 Pyridinone derivatives and pharmaceutical compositions thereof Pyridinone derivatives, process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related conditions in both men and women, as well as a mammal in general (also referred to herein as a "subject"). For example, such conditions include endometriosis, uterine fibroids, polycystic ovarian disease, heavy menstrual bleeding, particularly menorrahagia and dysmenorrehea, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to pyridinone derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
CN1879651A Eye drop containing micro-elements and preparation method thereof The invention relates to an eyedrops which can protect eye and treat eye disease, and relative preparation, wherein said preparation comprises: adding potassium, sodium, bisilicate, calcium, magnesium, strontium, and zinc into distilled water and/or pure water to be dissolved; or using the natural mineral water that contains bisilicate, calcium, magnesium, and strontium to be added with sodium, potassium, calcium and zinc to adjust the PH value to 6.1-7.2, to be fill into eyedrops bottle, to be sealed. The invention can treat eye fatigue, near sight and cataract, etc.
CN101250136A 1,3-diaryl-3-aryl amidine-1-acetoxime compounds, preparation method and use thereof The invention relates to a non-steroidal androgen receptor modulator compound containing 1, 3-diaryl-3-aromatic amine-1-acetoxime compound (I), or relative medical acceptable salt and a relative preparation method. The invention also relates to a drug compound of 1, 3-diaryl-3-aromatic amine-1-acetoxime compound (I) and relative medical acceptable salt. The1, 3-diaryl-3-aromatic amine-1-acetoxime compound (I) or relative medical acceptable salt has androgen receptor antagonistic activity, therefore, the compound can be used to prepare the non-steroidal drug for preventing or/treating prostatic hyperplasia, prostate cancer, hirsutism, serious androgen dependence alopecia and acne or the like.
CN1772761A Serial cyclovirobuxine compounds as new medicine for preventing and treating cardiac vascular diseases and their prepn The present invention discloses sulfamide derivatives of cyclovirobuxine capable of improving cardiac vascular function and their preparation process. These compounds have excellent effects of resisting arrhythmia and myocardial ischemia and tonifying the heart. They have plant active monomer cyclovirobuxine with cardiac vascular improving activity and are modified structurally based on molecular pharmacodynamics, so that they have high activity of improving cardiac vascular function.
DE102007027201A1 Conjugates useful for chemotherapy or positron emission tomography comprising a platinum complex and a glucose compound Conjugates comprising a chemotherapy-active platinum complex and a glucose compound, optionally linked together via a spacer, are new. - ACTIVITY : Cytostatic. No biological data given. - MECHANISM OF ACTION : DNA alkylating agent.
WO2009104005A1 Chronic wound treatment The invention provides the use of an unbound polyphosphate to promote chronic wound healing, in which the polyphosphate has at least 3 phosphate units. Also provided are a method of treatment and a pharmaceutical composition, both based on the use of the polyphosphate.
US7273854 Recombinant adenovirus, adeno-associated virus or herpes virus (especially a replication defective virus) containing a nucleic acid of a specific sequence encoding an antisense RNA that inhibits expression of p53. The present invention relates to pharmaceutical compositions that act on the p53 protein or its gene and methods of use for the treatment of neurodegenerative diseases.
WO2012073375A1 Novel compound, and kinesin spindle protein inhibitor and application thereof Provided is a compound characterized by being represented by general formula (I). In general formula (I): R1 and R2 may be the same or different and represent an optionally substituted alkyl group; and R3 represents a group represented by general formula (II) or general formula (III). In general formula (II) and general formula (III): X represents a hydrogen atom or a halogen atom; R4 represents a methyl group, a dimethyl group or an oxygen atom; and * represents a bond.
EP1674575A2 Ligand for herpes simplex virus entry mediator and methods of use A novel polypeptide ligand, p30, or LIGHT, for herpes virus entry mediator, HVEM, is provided. p30 is useful for modulating immune responses and in inhibiting infection and/or subsequent proliferation by herpes virus. HVEM fusion proteins are also provided. Methods for treating subjects with lymphoid cell disorders, tumors, autoimmune diseases, inflammatory disorders of those having or suspected of having a herpes virus infection, utilizing p30 and the fusion proteins of the invention, are also provided.
US20070244133 Thienopyrimidines and Thiazolopyrimidines for Use in Medicine The use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein X1, X2, X3, X4, Ra, p, R1, Z, Y, R2, R3 and R4 are as defined in the specification, in the preparation of a medicament for the treatment of C—C chemokine mediated conditions, such as inflammatory disease. Certain compounds of formula (I) are novel and these, together with their preparation are also described and claimed.
US20080280945 Crystalline forms of an HIV integrase inhibitor Crystalline forms of a hexahydro-diazocinonaphthyridine trione compound are disclosed. The compound and its crystalline forms thereof are HIV integrase inhibitors useful for the prophylaxis or treatment of HIV infection or for the prophylaxis, treatment or delay in the onset or progression of AIDS.
CN102327259A Composite biological preparation with obvious chemical hepatic injury protecting function The invention relates to a composite biological preparation with an obvious chemical hepatic injury protecting function, which consists of the following raw materials in weight ratio: 15-18 parts of glycine, 12-15 parts of arginine, 15-18 parts of cysteine, 16-18 parts of glutamine, 7-10 parts of S-adenosylmethionine and 7-12 parts of alpha-lipoic acid. The composite biological preparation has favorable therapeutic action and prevention action to all hepatic injury caused by various reasons, and has the effective rate (effectual rate) of 98.6% and the cure rate of 76.8%.
EP1743635A2 Gibberellins for the promotion of ulcer healing Compounds of formula (1) (Gibberellins), and their pharmaceutically acceptable derivatives when used as promoters of lesion-healing, ulcer-healing, wound-healing or cultivation of skin cell lines or hair growth on animals, including humans, wherein A is COOR, where R is hydrogen, unsubstituted or substituted C1-20 alkyl, allyl, aryl, arylalkyl, amidine, NR4R5 or an unsaturated or saturated ring containing one or more heteroatoms. R4 and R5 may or may not be the same, are hydrogen, or C1-20 alkyl, allyl, aryl, aralkyl or an unsaturated or saturated ring containing one or more hetero-atoms; B is hydrogen, hydroxyl, mercaptan, halogen; or A and B together form a -CO-O- linkage; R1 is hydrogen, hydroxyl, mercaptan, halogen, amino, azido, NR4R5, unsubstituted or substituted C1-20 alkyl, allyl, aryl, arylalkyl; and R2 is methylene, hetero-atoms.
WO2011057108A1 Ophthalmic formulations containing substituted gamma lactams and methods for use thereof The invention provides ophthalmic formulations containing well-defined substituted gamma lactams. The formulations described herein are useful in treating a variety of ocular diseases related to ocular hypertension, such as for example, glaucoma.
WO2011002001A1 Combined medicine of pyrazole derivative and biguanide drug Disclosed is a novel medicinal agent useful for the treatment of hyperglycemia-related diseases or the like. Specifically disclosed is a medicinal agent useful for the treatment of hyperglycemia-related diseases or the like, which comprises a combination of 3-(3-{4-[3-(β-D- glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3- methylphenoxy}propylamino)-2,2-dimethylpropionamide, which has an inhibitory activity on SGLT1 (sodium-dependent glucose cotransporter 1), or a pharmacologically acceptable salt thereof and a biguanide drug such as metformin.
US7790712 and Mitogen-Activated Protein Kinase-Activated Protein kinase-2 (MAPKAP-k2 inhibitors, used for preventing or treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease The application relates to compounds of formula Ia and analogues thereof wherein R1 to R13 and X are as defined herein. The invention also relates to the use of the compounds of formula Ia as inhibitors of Mitogen-Activated Protein Kinase-Activated Protein kinase-2 (MAPKAP-k2), and also to a method for preventing or treating a disease or disorder that can be treated or prevented by modulating the activity of MAPKAP-K2 in a subject and to pharmaceutical compositions and kits that include these MAPKAP-K2 inhibitors.
CN102477032A 2-cyclopropyl-4-substituted-phenoxy-quinoline derivatives, and its preparation method, intermediate and application The invention discloses 2-cyclopropyl-4-substituted-phenoxy-quinoline derivatives as represented by formula A, and its preparation method, intermediate and application. The 2-cyclopropyl-4-substituted phenoxy-quinoline derivatives provided in the invention have good activity in inhibiting HMG-CoA reductase and can be used for preparing medicines which can inhibit HMG-CoA reductase or treat diseases related to hyperlipidemia. In formula A, R1 is H or halogen, R2 is H, halogen, C1-C4 alkoxy groups or a group as represented by formula Q, R3 is H, halogen, or a group as represented by formula Q, and R4 is a group as represented by formula Q, wherein, in formula Q, R is H, halogen, C1-C4 alkyl groups or C1-C4 alkoxy groups.
WO2006105796A1 Novel indolinone derivatives The invention relates to novel indolinone derivatives of formula (I), wherein X, R1, R2, R3, R4, R5, Re, Ri', Ri , FV/ R4'/ FV and R6' are as shown herein, as well as their use in the treatment of inflammatory autoimmune diseases, in particular by administration via the oral route.
CN102653534A Lignans compound of aromatic tobacco and preparation method and application of lignans compound The invention discloses a lignans compound in an aromatic tobacco, a preparation method for the lignans compound and application of the lignans compound, belongs to the chemical field of tobaccos, and in particular relates to a 7,8-breakage lignans compound in a novel aromatic tobacco, a preparation method for the lignans compound, a function for protecting human immunodeficiency virus (HIV) infection cells and a function poisoning the cells. The 7,8-breakage tobacco lignan (I) is prepared by smashing an aromatic tobacco in Yunnan Baoshan, performing ultrasonic extraction on the smashed aromatic tobacco by 95 weight percent of ethanol repeatedly, combining extracts, decompressing and concentrating to obtain an extract, initially dividing the extract by silica gelcolumn chromatography and further separating by high performance liquid chromatography. The compound has a simple structure, is artificially synthesized easily and remarkable in HIV-1 resistant activity and can be used as a pilot compound for developing an anti-HIV medicine.
US6867225 Alpha type human peroxisome proliferator activated receptor agonists; such as 2-methyl-2-(3-methyl-4-(((4-phenoxymethyl-2-(4-trifluoromethylphenyl) -thiazol-5-yl-carbonyl)-amino)-methyl)phenoxy)propionic acid A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof Wherein R1 and R2 are independently H or C1-3 alkyl or R1 and R2 which are bonded to the same carbon atom may together with the carbon atom to which they are bonded form a 3-5 membered cycloalkyl ring; X1 represents O or S; Each R3, R4, R8 and R9 independently represents H, halogen, —CH3 and —OCH3; R5 represents H or C1-6 alkyl or R4 and R5 together form a 3-6 membered cycloalkyl ring. X2 represents NH, NCH3 or O; One of Y and Z is N, and the other is O or S; R6 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one or more halogen, CF3, C1-6 straight or branched alkyl (optionally substituted by halogen), with the provision that when R6 is pyridyl, the N is unsubstituted. R7 represents C1-6alkyl, (optionally substituted by one or more halogens), —C0-8alkyl-5 membered heteroaryl, C0-6alkyl-(O)n-phenyl, wherein n is 0 or 1, with the proviso that when R1 and R2 are methyl, R8 and R9are H, R5 is H, then R7 cannot be CH3 or CF3.
CA2393518C Amycomycin, a process for its production and its use as a pharmaceutical A compound named Amycomycin of formula (I) and its pharmaceutically acceptable salts and derivatives, in all their stereoisomeric and tautomeric forms is obtainable by cultivation of the microorganism Amycolatopsis sp., ST101170 (DSM 12216) and finds use a pharmaceutical, particularly as an antibiotic.
EP0832227B9 Method for prolonging the expression of a gene of interest using soluble ctla4 molecules The invention provides a method for enhancing the expression of a gene of interest by a cell, the cell (a) comprises a recombinant nucleic acid sequence encoding and (b) is capable of expressing the gene of interest, the method comprising contacting the cell with an amount of a soluble CTLA4 molecule effective to enhance the expression of the gene of interest by the cell.
US20130065878 Cell-free preparation of carbapenems Provided herein are cell-free systems for generating carbapenems, e.g., a compound of the Formula (I): or salts thereof; wherein , R1, R2, R3, R4, R5, and R6 are defined herein. Also provided are pharmaceutical compositions comprising a compound generated by the inventive cell-free system, and use of these compounds and compositions for the treatment of bacterial infections.
EP1127057B1 Naphthyridine compounds and thier azaisosteric analogues as antibacterials Piperidine derivatives of formula (I) or a pharmaceutically acceptable derivative thereof and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
CA2072785C Pharmacologically active hydrazine derivatives and processes for the preparation thereof The invention relates to compounds of formula (see formula I) wherein R1 and R9 are each independently of the other hydrogen; aryl; unsubstituted or substituted alkyl, alkenyl or alkynyl; heterocyclyl; sulfo; sulfonyl substituted by unsubstituted or substituted alkyl, aryl, heterocyclyl, alkoxy, which is unsubstituted or substituted, or by aryloxy; sulfamoyl that is unsubstituted or substituted at the nitrogen atom; or phosphoryl substituted by one or two radicals, which may be identical or different, selected from unsubstituted or substituted alkyl, from unsubstituted or substituted cycloalkyl, from aryl, from hydroxy, from unsubstituted or substituted alkoxy, from cycloalkoxy and from aryloxy; with the proviso that not more than one of the radicals R1 and R9 is hydrogen; and R2 and R8 are each independently of the other hydrogen or one of the radicals mentioned above for R1 and R9; or the pairs of substituents R1 and R2, and R8 and R9, each independently of the other, may form together with the nitrogen atom to which they are bonded certain heterocyclic rings;R3 and R4 are each independently of the other hydrogen; unsubstituted or substituted alkyl or cycloalkyl; aryl; heterocyclyl; or unsubstituted or substituted alkenyl; or R3 and R4 together form unsubstituted or substituted alkylene, alkylidene or benzo-fused alkylene; R5 is hydroxy; R6 is hydrogen;or R5 and R6 together are oxo; and R7 is unsubstituted or substituted alkyl or cycloalkyl; aryl; heterocyclyl; or unsubstituted or substituted alkenyl;and salts of the mentioned compounds where salt-forming groups are present, and to processes for the preparation thereof, to pharmaceutical compositions, to the use thereof as medicaments or for the preparation of pharmaceutical compositions, and to novel intermediates for the preparation of those compounds.
EP2127661A1 Probiotics to improve gut microbiotica The use of probiotic bacteria in the manufacture of a medicament or therapeutic nutritional composition for promoting the development of an early bifidogenic intestinal microbiota in infants without siblings.
US20110130450 Pravastatin extraction The present invention provides a method for the purification of pravastatin comprising extracting a solution comprising pravastatin in a water-immiscible solvent with water at a pH value ranging from 5.0 to 7.0.
US20100168029 Methods for treating bone tumors The present invention provides methods of treating bone cancer, inducing differentiation of bone tumor cells, inhibiting bone tumor growth, inducing bone tumor regression or treating a hyperproliferative cell disorder by administering a pharmaceutically effective amount of a bone morphogenic protein or a nucleic acid encoding the bone morphogenic protein.
WO2011124430A1 Tricyclic indazole compound, method of preparation and pharmaceutical composition containing it Tricyclic indazole compound and its pharmaceutically acceptable salts of acid addition, use thereof, method and intermediates for preparing them, and a pharmaceutical composition containing them. The tricyclic indazole compound has the following general Formula (I): in which R1, R2, L1, L2, X1, X2, X3, X4, X5, Y, W, m, and n have the meanings stated in the description.
CN101108867A 1-0-caffeoyl -6-0-(S)-caesalpinia sepiaria acyl group -Beta-D-glucopyranose and uses thereof The invention provides condensed tannin of the glucopyranose containing caffeoyl, in particular to the 1-O-caffeoyl-6-O-(S)-caesalpinia digyna acyl-Beta-D-glucopyranose. The chemical structure is as shown in the formula (I). The compound of the invention can inhibit the multiplication of the tumour and has better antitumor activity, which can be used for preparing the antitumor drugs.
CN103172540A Phenylglycine histone deacetylase inhibitor as well as preparation method and applications thereof The invention belongs to the technical field of pharmaceutical chemistry, and particularly relates to a phenylglycine histone deacetylase inhibitor as well as a preparation method and applications thereof. The invention provides a superactive histone deacetylase inhibitor, which relates to a compound with a structure shown in the general formula (I), and also relates to various optical isomers thereof, a pharmaceutically acceptable salt, a solvate and a prodrug. The invention also relates to a pharmaceutical composition containing the compound with a structure shown in the formula (I), and pharmaceutical applications thereof. According to the invention, diseases with abnormal histone deacetylase activity expression can be effectively treated.
EP1706109A1 Isoflavone therapy for treating urinary incontinence A method for treating urinary incontinence while reducing or eliminating undesirable side effects associated with conventional treatments involves administering to an animal in need of treatment an effective amount of an isoflavone compound.
US20110268787 Ocular compositions containing dioleoylphosphatidylglycerol and uses thereof The present invention provides a method of treating a corneal disorder comprising administering to a patient in need thereof a composition containing pharmaceutically effective amount of dioleoylphosphatidylglycerol and/or palmitoyloleoylphosphatidylglycerol and a pharmaceutically acceptable carrier.
WO2006073172A1 12-oxy-13-amino-containing 16-membered cyclic macrolide derivative and process for producing the same A compound represented by the following general formula (I) [wherein R1, R2, and R3 each independently represents hydrogen or alkylcarbonyl; and R4 and R5 each independently represents hydrogen, optionally substituted alkyl, optionally substituted aralkyl, optionally substituted heterocycle-alkyl, or optionally substituted heterocycle-alkenyl] or a pharmaceutically acceptable salt thereof.
CA2438657C Testosterone-containing transdermal therapeutic system and process for its production A transdermal therapeutic system for administering sex hormones which is provided with an active substance-impermeable backing layer, a pressure-sensitive adhesive polymer matrix connected therewith and containing a sex hormone as well as skin penetration-enhancing substances, and with a protective layer detachable prior to application, is characterized in that said polymer matrix contains the sex hormone testosterone as well as a mixture of at least one penetration-enhancing substance from the group comprising fatty alcohol esters and fatty acid esters, and at least one readily volatile penetration-enhancing substance.
US7485656 Fluconazole, a compound selected from a group consisting of fatty acid, fatty alcohol, higher fatty acid ester and lower alcohol and a base; favorable absorption and delivery through the human skin; low skin stimulation; stability; spreading An antibacterial composition for external application, particularly, a remedial formulation for external use containing fluconazole is disclosed. The formulation comprises a base material, 0.1-5.0 percent by weight of fluconazole and 1.0-40.0 percent by weight of any one compound selected from a group consisting of fatty acid, fatty alcohol, higher fatty acid ester and lower alcohol based on weight of the base material. The composition according to the present invention has various advantages of a favorable absorption into a system through the skin of a human body and delivery of active material into horny layer of the skin, a reduced skin stimulation and an excellent stability. Therefore, the composition is efficiently useable in a medical treatment application for dermatomycosis-related infectious diseases including tinea pedis, tinea corporis, tinea cruris, tinea versicolor and/or candidiasis and the like.
US20090197855 Pharmaceutical compositions of cefdinir A chewable tablet dosage form comprising Cefdinir or pharmaceutically acceptable salts thereof for the oral administration of Cefdinir in a manner that is more palatable and less objectionable to population group's especially young children and older patients. A method of preparing the chewable tablets comprising Cefdinir and method of treatment using the same.
CN1579388A New use of sulpirde in pharmacy The invention discloses the application of sulpiride in curing or preventing neurotoxicity caused by 3,4 methylene dioxygen methyl Benzedrine (MDMA). It feeds sulpiride to write rat before feeding MDMA, feeds sulpiride to experiment write rat when feeding MDMA to it, and feeds sulpiride to write rat half hours, five hours and twelve hours after feeding MDMA to it, it can reduce the exaust of brain areas 5-HT of frontal lobe cortex, hippocampal sulcus and corpus striatum, and has prominent resisting effect to the lessen of SERTmRNA representation; the result of neuropathology displays: the sulpiride also can resist the reduction of silver staining positive area caused by MDMA, and lessens the representation of gelatinous fiber acid protein (GFAP), this reflects the lessen of damage to the nerve. The dose of the sulpiride is 40mg/kg-80mg/kg.
US20110171187 Dietary supplements for promotion of growth, repair, and maintenance of bone and joints The present invention provides a dietary supplement that promote the growth, repair, and maintenance of mammalian bone and joint connective tissue. In particular, the dietary supplement comprises a combination of at least one metal chelate and at least one chondroprotective agent.
WO2005084684A1 Use of a mixture for the production of an agent for treating defective or degenerated cartilage in the production of natural cartilage replacement in vitro A mixture of one or several substances from group A) lubricin, proteoglycan 4 (PRG4) and phospholipid (SAPL); with one or several substances from group B) hyaluronic acid, glycosaminoglycan and derivatives of said substances; dissolved in a solvent, used for the production of an agent for treating defective or degenerated cartelage in vivo. Said mixture can also be used to produce natural cartilage replacement in vitro.
WO2010014771A1 Romazarit for treating metabolic diseases A method for treating a condition of low metabolic rate, dyslipidemia, excess adiposity and/or insulin resistance, or a disease or syndrome characterized by one or more of said conditions in a subject, comprises administering to the subject a therapeutically effective amount of romazarit or a pharmaceutically acceptable salt, ester or prodrug thereof.
CN101016270B Substituted piperazinphenylisoxazoline derivative and use thereof The invention belongs to the infection relevant medicine fields, and provides a substituted piperazine phenyl isoxazoline derivant with a structure as general formula (1) and pharmaceutical acceptable salt, wherein R1 is amino, and amino mono-substituted or disubstituted by C1-6 alkyl, -N=C, and -N=R7; R2 is H, and C1-C6 alkyl; R3 is H, F, and Cl; R4 is C1-C6 alkyl and C1-C6 alkyl mono-substituted or polysubstituted by halogen; R5 and R6 are H, C1-C6 alkyl and substituted C1-C6 alkyl, heterocycle, and substituted heterocycle; R7 is C3-C6 cycloalkyl, substituted C3-C6 cycloalkyl, C3-C6 cycloalkyl with S, O and aza-atom, substituted C3-C6 cycloalkyl with S, O and aza-atom, C3-C6cycloalkyl aryl, and substituted C3-C6 cycloalkyl aryl. The invention also provides the compound or pharmaceutical acceptable salt as a drug, especially the use as antibiotic medicine.
WO2008133952A2 Transmucosal treatment with fentanyl in patients with mucositis In accordance with the invention is an fentanyl-containing dosage form designed for transmucosal delivery which includes both an effervescent couple and a pH adjusting substance which can be administered to patients suffering from both pain and mucositis. Also provided is a method of treating pain in a patient having mild oral mucositis by administering a fentanyl-containing dosage form designed for transmucosal delivery.
CN101322743A Formulation capable of repairing lesion and damnification of eye and improving asthenopia and preparation thereof The invention relates to a preparation which can repair pathological injuries of eyes and relieve asthenopia and a preparation method thereof. The preparation is prepared by xanthophyll, taurine, pearl powder, natural carotene, cyanidin, vitamin C, vitamin B1, B2, B6, B12, vitamin E, folic acid and alpha-linolenic acid oil. The preparation method is that the xanthophyll extract is prepared first; the xanthophyll extract, taurine, pearl powder and natural carotene are mutually mixed; cyanidin, vitamin C, vitamin B1, vitamin B2, vitamin B12, vitamin E, alpha-linolenic acid oil and folic acid oil are mixed, distilled by a flask and a condenser tube and added with auxiliary materials to make into a soft capsule. The preparation of the invention can provide nutrition required by eyes, relieve asthenopia, improve microcirculation, protect health of ocular capillary blood vessel, relieve intraocular pressure, nourish optic nerves, clear away poisonous substances in retina, inhibit and remove pathogenic factor in eyes and maintain eye health, which is used for improving various ophthalmic diseases such as eyesight worsening, glaucoma, cataract, etc.
CN1903183A Dispersion tablets of telbivudine and its prepn. method A dispersing tablet of Tibifuding is prepared from Tibifuding and the medicinal carrier chosen from disintegrant, filler, surfactant, wet adhesive and lubricant through wet granulating and tabletting.
EP1797876A1 Combinations of vasoactive agents and their use in the treatment of sexual disfunctions This invention relates to combinations of vasoactive substances which are useful in the treatment of sexual dysfunctions associated with poor local blood supply and/or insufficient lubrication. The active compounds are selected from a: - esculoside or visnadine; - forskolin or extracts containing it, or alternatively, purified lipophilic extracts of plants of the genus Ipomea; - esters of ximenynic acid; - optionally, at least one compound selected from a icarin or derivatives or extracts thereof which contain it, amentoflavone, and Gingko biloba dimeric flavones. The combination of these vasoactive substances is incorporated in gels and lotions designed to be applied to the genital organs. These formulations are useful in inducing erection of the male and female sex organs and enhancing orgasm and sexual performance. The formulations are particularly useful in the treatment of female sexual dysfunctions.
US20100010066 Optimized Methods For Delivery Of DSRNA Targeting The PCSK9 Gene This invention relates to optimized methods for treating diseases caused by PCSK9 gene expression.
CN103156832A Application of 3-mercaptopropionic acid compounds in inhibiting NDM-1 The invention provides an application of 3-mercaptopropionic acid compounds preparing drugs for inhibiting activity of drug-resistant bacteria, wherein the structural formula of the 3-mercaptopropionic acid compounds is as follows, wherein R represents a C1-C3 alkane or a C1-C4 alkyl group with a cyclic structure. The compound provided by the invention has very good effect for inhibiting the activity of NDM-1. An IC50 value for inhibiting the activity of the NDM-1 of the compound 2-methyl-3-mercaptopropionic acid is 56.3 +/- 10.9 [mu]M.
EP1889615A2 Formulations for oral administration with a health promoting effect on the osteoarticular and muscleskeleton apparatus A pharmaceutical composition or dietary supplement or another preparation suitable for oral administration, having health promoting effects on the joints and the musculoskeletal apparatus, comprising glucosamine or a simple or mixed salt thereof, preferably in the form of crystalline glucosamine sulphate, and mangostin, preferably in the form of an extract of Garcinia mangostana fruit. Thanks to a combination of activities, such as that of stimulating trophism and protecting joint cartilage and an anti-inflammatory activity towards musculoskeletal tissues, the association of the aforementioned active agents may be used to obtain health promoting effects for maintaining osteoarticular wellbeing and for the prevention and treatment of degenerative or inflammatory disorders of the osteoarticular or musculoskeletal apparatus.
US8716348 Formoterol/steroid bronchodilating compositions and methods of use thereof Bronchodilating compositions and methods are provided. The compositions are intended for administration as a nebulized aerosol. In certain embodiments, the compositions contain formoterol, or a derivative thereof, and a steroidal anti-inflammatory agent. Methods for treatment, prevention, or amelioration of one or more symptoms of bronchoconstrictive disorders using the compositions provided herein are also provided.
EP1609467A1 Compositions for treating diseases associated with glycosaminoglycan-associated molecular interactions Therapeutic compounds and methods for inhibiting a glycosaminoglycan (GAG)-associated molecular interaction in a subject, whatever its clinical setting, are described.
US20090239917 Heterocyclic Cycloalkyl Compounds, a Process for their Preparation and Pharmaceutical Compositions Containing Them Compounds of formula (I): wherein: R1 represents a (C3-C8)cycloalkyl group, R2 represents a group of formula (II) as defined in the description, X represents an oxygen atom or an N—OR′ group wherein R′ represents a hydrogen atom, a linear or branched (C1-C6)alkyl group, an aryl group or an aryl-(C1-C6)alkyl group in which the alkyl moiety may be linear or branched. Medicinal products containing the same which are useful as hypoglycaemic and hypolipaemic agents.
EP1816123A1 Intermediates for the production of pharmaceutically active compounds The present invention provides a compound of a formula (A), (B) or (C): which is useful for making a compound of formula (I): wherein Z is CO2R3. The compounds of formula (I) are useful in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
EP2474312A1 Means for topical treatment of skin ailments Agent (I) comprises (a) 0.1-90 wt.% of coal tar solution, (b) 0.1-40 wt.% of finely divided sulfur, (c) optionally a liquid or solid carrier or diluent and (d) hydantoin and/or its derivative. - ACTIVITY : Antipsoriatic; Dermatological. - MECHANISM OF ACTION : None given.
CN102626388A Liposome solid preparation of ozagrel The invention discloses a liposome solid preparation of ozagrel and a preparation method thereof. In the invention, an active ingredient ozagrel hydrochloride and a special combination of hydrogenated yolk lecithin, dioleoyl-phosphatidyl-ethanolamine, cholesteryl succinate, and Span 20 are prepared into a liposome, thereby greatly improving stability, dissolubility, and bioavailability of the drug, and having stable and lasting effect and obvious curative effect. According to the invention, product quality of the preparation is improved, and the toxic side effect is reduced.
US20120251514 Modulated programmed death ligand-1 The invention provides nucleic acids comprising a nucleotide sequence encoding programmed death ligand-1 (PD-L1) and a nucleotide sequence encoding a fusion protein comprising thymidylate kinase (TMPK) or a variant thereof and a cell surface marker or a variant thereof. Recombinant expression vectors, host cells, populations of cells, pharmaceutical compositions, and kits relating to the nucleic acids are disclosed. Methods of treating or preventing a disease in a host and methods of suppressing an immune system in a host are also disclosed.
US20050209198 Pharmaceutical composition comprising a bisphosphonate and a cox-2 inhibitor for the treatment of bone diseases A pharmaceutical composition for treatment of conditions of abnormal bone turnover, comprises in combination a bisphosphonate and a COX-2 inhibitor for simultaneous, sequential or separate use. Also provided is a method of treating a patient suffering from a condition involving abnormal bone turnover, comprising administering to the patient an effective amount of a bis-phosphonates and an effective amount of a COX-2 inhibitor.
CN101909630A Methods and compounds for preventing and treating a tumour The invention relates to a method of preventing, inhibiting, arresting or reversing tumourigenesis in a cell as well as a method of inducing apoptosis in a tumour cell. The method includes increasing the amount and/or the activity of a DACT protein, or a functional fragment thereof, in the cell. Also provided is a pharmaceutical composition that comprises a compound of general formula (I), wherein A is CH or N, R1, R4 and R5 are independent from each other H, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group comprising 0 - 3 heteroatoms. The heteroatoms may be N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen such as F, Cl, Br or L. R3 is H, F, Cl or an aliphatic or arylaliphatic group that includes 1 - 8 main chain carbon atoms and 0 - 3 heteroatoms. The pharmaceutical composition also comprises a histone deacetylase inhibitor.
WO2006004574A2 Method for using gamma cyclodextrin to control blood glucose and insulin secretion Disclosed are methods of producing a blunted postprandial glycemic response in an individual, and/or reducing postprandial insulin secretion, said methods comprising administering to the individual a nutritional or other product comprising gamma-cyclodextrin. Also disclosed are similar other methods directed toward the use of such products to provide weight and appetite control, to normalize blood glucose levels in individuals with impaired glucose tolerance, to minimize nighttime hypoglycemia in diabetic and non-diabetic patients, to prevent reactive hypoglycemia in susceptible non-diabetics, to normalize blood glucose levels in individuals with gestational diabetes or impaired glucose tolerance during gestation, and/or to provide a prolonged glycemic response during exercise. The methods are based upon the discovery that gamma-cyclodextrins are rapidly metabolized and absorbed in the small intestine, but subsequently result in a surprisingly blunted postprandial glycemic response and reduced insulin secretion.
WO2008061016A1 N-substituted piperidinyl 4 -arylsulfonamides as modulators of the secreted frizzled related protein- 1 Compounds of formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. and pharmaceutically acceptable salt thereof, which are modulators of secreted frizzled related protein-1, are disclosed. The compounds, and compositions containing the compounds, can be used to treat various diseases and disorders, including osteoporosis, arthritis, chronic obstructive pulmonary disease, cartilage defects, bone fractures, leiomyoma, acute myeloid leukemia, wound healing, prostate cancer, autoimmune inflammatory disorders, such as Graves ophthalmopathy, and combinations thereof.
CN102078328A Use of potassium ferricyanide in preparing medicine for inhibiting tumor cell metastasis The invention discloses a medicine K3 [Fe(CN)6] capable of effectively inhibiting tumor cell metastasis; the cell experiment is done on the K3 [Fe(CN)6] with extraordinarily excellent 50% inhibitory concentration in preliminary screening of zymologic experiment, and the result shows that the K3 [Fe(CN)6] has quite small impact on the viability of HT1080 cell which has the cell viability above 80% within the concentration range of 100mum, and under low administration conditions, the K3 [Fe(CN)6] has relatively significant inhibiting effect on the metastasis ability of cells. In the cell metastasis experiment, the cell metastasis ability is prominently impacted at the administration concentration of 10mum. The result shows that the K3 [Fe(CN)6] has excellent inhibiting effect on tumor cell metastasis and is expected to be further developed into an antitumor medicine.
CN103271901A Application of dihydromyricetin (DHM) in preparation of anti-hepatoma medicines The invention relates to the biological medicine field, and concretely relates to an application of DHM in the preparation of anti-hepatoma medicines. The DHM has a strong anticancer characteristic as a flavonoid compound. Tests prove that the DHM plays a positive role in hepatoma carcinoma cell propagation inhibition, hepatoma carcinoma cell apoptosis induction, hepatoma carcinoma cell adhesion capability reduction and hepatoma carcinoma cell invasion and transfer prevention, and can substantially reduce the contents of peroxides, glutathione and ATP in the hepatoma carcinoma cells.
EP1965800B1 Piperidine derivatives for use to treat incontinences The invention relates to the fields of pharmaceutical chemistry and pharmacological treatments. More specifically, the invention relates to compositions and methods for the treatment of incontinence, voiding disorders associated with lower urinary tract dysfunctions and/or and urethro-vesical and anal sphincteral disorders. The invention can be used, for example, for the treatment of pollakiuria, urinary urgency, nocturia or enuresis, true faecal incontinence, functional faecal incontinence (FFI), passive faecal incontinence, faecal urgency and/or faecal seepage. The invention is suitable for preventive or curative use with all mammals, particularly humans.
CN103006619A Patch for heroin addiction withdrawal, preparation method and application thereof The invention discloses a patch for heroin addiction withdrawal, a preparation method and an application thereof. The patch for heroin addiction withdrawal of the invention comprises a backing layer, a substrate layer, and a protection layer; the substrate layer of the patch comprises a main drug effective component of naltrexone hydrochloride, wherein naltrexone hydrochloride accounts for 30-55 wt% of the substrate layer; the substrate layer comprises 45-70 wt% of a film forming slow release carrier; the slow release carrier is acrylate copolymer. The patch for heroin addiction withdrawal of the invention is used for pasting on human body abdominal navel, adopts a mechanism method of percutaneous forced automatic drug administration, employs a therapy of psychological dependence resistance, has no side effect, and allows patients to work and study as normal people during detoxification process.
EP2493481A1 Anti-cancer composition comprising alginate The present invention relates to a biologically acceptable composition for the prophylaxis and/or treatment of colorectal cancer comprising an iron chelator, wherein the composition is adapted for the selective targeting of the iron chelator to the colon.
WO2013149102A1 Compositions comprising scopolamine and ketamine in the treatment of depression Described are compositions and methods for administering scopolamine and ketamine in the treatment of depression (e.g., Major Depressive Disorder and Treatment-Resistant Depression).
US7078389 Hybridization of a mutagen substituted single-strand nucleic acid molecule with DNA causes a mutation at a specific site; antiproliferative and anticarcinogenic agents; gene therapy A mutagenic, triplex-forming oligonucleotide and methods for use thereof wherein the oligonucleotide is chemically modified to incorporate a mutagen and forms a triple-stranded nucleic acid molecule with a specific DNA segment of a target DNA molecule. Upon formation of the triplex, the mutagen is brought into proximity with the target molecule and causes a mutation at a specific site therein. The mutation activates, inactivates or alters the activity and function of the target molecule.
CN102000191A Ulcer removing powder used for treating oral cavity and throat ulcer The invention provides ulcer removing powder used for treating oral cavity and throat ulcer, which is prepared from the following raw materials in parts by weight: 5-10 parts of Rheum officinale Baill., 5-10 parts of rhizoma coptidis, 5-10 parts of Phellodendron chinense Schneid, 10-15 parts of realgar, 8-15 parts of cinnabar, 10-15 parts of borax, 1-5 parts of bluestone, 11-16 parts of indigo naturalis, 9-14 parts of dried alum, 1-7 parts of rhinoceros horn, 0.5-1.5 parts of calculus bovis and 9-14 parts of borneol. The ulcer removing powder is used for treating dental ulcer, oral herpes, oral erosion, angular stomatitis, gingivitis, throat fester, throat herpes, pharyngeal diphtheria, mycotic stomatitis, tonsillitis, pharyngitis, oral and throat herpes and ulcer caused by the young child hand-foot-mouth disease; by adopting the technical schemes of clearing heat and removing dampness, detoxicating and diminishing inflammation, nourishing the yin and promoting tissue regeneration, astringing and relieving the pain, the ulcer removing powder achieves the purpose of treating both principal and secondary aspect of diseases; the ulcer removing powder has the advantages of less dosage, short course of treatment, quick effect taking and no side effects; and the ulcer can be cured within 1-2 days for the patients with lighter symptoms, and the effective rate of the ulcer removing powder is 100 percent.
US20100061981 p75NTR MEDIATES EPHRIN-A REVERSE SIGNALING The disclosure comprises methods and compositions for stimulating axon outgrowth and inhibiting metastatic diseases and disorders.
US7429584 Furo[2.3-b]pyridine derivatives for the treatment of hyper-proliferative disorders This invention relates to a compound of Formula (I) wherein Y is CH or N; Ar1 is phenyl or pyridyl each optionally substituted with 1 or 2 substituents each selected independently from (C1-C3)alkoxy halo, OH, CF3, CN, NO2 and (C1-C3)alkyl, said alkyl being optionally substituted with CF3; Ar2 is phenyl or pyridyl each optionally substituted with 1 or 2 substituents each independently selected from halo, OH, CN, NO2, CF3, (C1-C6)alkoxy, NR1R1, S(O)2R2, C(O)R3, and (C1-C6)alkyl optionally substituted with R4, and its use in treating hyper-proliferative disorders.
EP1289557B1 Cancer treatment composition containing an anti-neoplastic agent and a pde4 inhibitor The invention relates to a method for treating cancer including administering to a mammal therapeutically effective amounts of an anti-neoplastic agent and a PDE4 inhibitor, treatment combinations containing the same as well as a method for attenuating unwanted cancer treatment side effects including myelosuppression and mucositis.
US20100029734 Methods for breast cancer screening and treatment A method for selecting a breast cancer patient for therapy with an agent that reduces production of angiotensin II, for example an ACE inhibitor or renin inhibitor, comprises (a) determining whether the cancer comprises a tumor that is estrogen receptor positive (ER+) and (b) selecting the patient for such therapy only if the cancer is determined to comprise an ER+ tumor. A method for treating breast cancer in a patient further comprises (c) administering to the patient, if so selected, an agent that reduces production of angiotensin II, for example an ACE inhibitor or renin inhibitor. A method for treating a breast tumor in a patient having SERM-resistant ER+ breast cancer comprises administering to the patient an agent that reduces production of angiotensin II, for example an ACE inhibitor or renin inhibitor. A therapeutic combination useful in treatment of a breast tumor comprises an agent that reduces production of angiotensin II, for example an ACE inhibitor or renin inhibitor, and a second agent that comprises (a) an aromatase inhibitor or (b) an estrogen receptor modulator or antagonist.
WO2006040149A1 Heterocyclic ketone compounds for treating alzheimer’s disease The present invention relates to novel ketone compounds' of formula (I) wherein, inter alla, A-B represents -NR5p'SO2-; -W- represents -CH2-, -(CH2)2-, -(CH2)3- or -C(H)=C(H)-; X-Y-Z represents -C=CR8-NR9-, having Asp2 (ß-secretase, BACE1 or Memapsin-2) inhibitory activity, processes for their preparation, to -compositions containing them and to their use in the treatment of diseases characterised by elevated ß- amyloid levels or ß-amyloid deposits, particularly Alzheimer's disease.
US20130059851 Methods of Diagnosing and Treating Cancer in Patients Having or Developing Resistance to a First Cancer Therapy A method of identifying a subject having cancer who is likely to benefit from treatment with a combination therapy with a RAF inhibitor and a second inhibitor is provided. A method of treating cancer in a subject in need thereof is also provided and includes administering to the subject an effective amount of a RAF inhibitor and an effective amount of a second inhibitor, wherein the second inhibitor is a MEK inhibitor, a CRAF inhibitor, a CrkL inhibitor or a TPL2/COT inhibitor. A method of identifying a kinase target that confers resistance to a first inhibitor is also provided.
WO2010066046A1 Proliferation-associated modulation of the splicing of the integrin alpha 6 isoforms This application relates to the use of agents such as expression vectors and nucleic acids encoding integrins α6 A or α6B as well as antibodies specific for those integrins which are capable of modulating the ratio between the B and A isoforms of the α6 integrin in the treatment of diseases associated with an altered proliferation rate, such as cancer. The application also relates to the use of the ratio between the B and A isoforms of the α6 integrin in the diagnosis of diseases associated with an altered proliferation rate.
CN101152197A Compound glycyrrhizin dropping pills and method for preparing the same The invention relates to a compound glycyrrhizic glycoside dropping pill and the preparation method. Each granule of the compound glycyrrhizic glycoside dropping pill of the invention contains the following portion of active components: 1 to 25mg of glycyrrhizic glycoside, 1 to 25mg of medhionine and 1 to 25mg of glycine; and the following pharmaceutically acceptable components: 5-100mg of medium, 0 to 0.09mg of surfactant and 0 to 0.08mg of taste masking agent. The preparation method of the invention is: formula dose of the medium of the dripping pill is heated and melted, and then is added in with surfactant and stirred uniformly; formula dose of uniform mixture of glycyrrhizic glycoside, DL-methionine and glycine are added once or at several times; taste masking agent is added in, stirred uniformly, preserved under conditions between 70 to 80 degrees centigrade; the melted liquid is added dripped in condensing agent at a speed of 10 to 100 drops a minute; when the dropping pill is cooled and shaped, the condensing agent is trickled. After qualification test, the finished product is prepared.
CN101455628B Preparation method of gel composition for eyes The present invention discloses an ophthalmic gel composition and a preparing method thereof, wherein the ophthalmic gel composition according to the invention is composed of chondroitin sulfate, taurine and medical supplementary material. The invention successfully develops the ophthalmic gel composition which is currently hard through combining the prior clinical ophthalmic medicine. The ophthalmic gel composition has excellent fluidity and dispersibility and has beneficial contribution for increasing curative effect. Furthermore the prior animal experiment shows that the ophthalmic gel composition of the invention has excellent safety and provides a powerful guarantee for the further product commercialization.
US20090028815 Diazabenzo[De]anthracen-3-one Compounds and Methods for Inhibiting Parp The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.
CN101406543A Technique for preparing oral liquid for cough and asthma of children The invention relates to a preparation technique for children cough oral liquid, which comprises the following steps in turn: (1) extracting primary liquid medicine; (2) purifying the primary liquid medicine to obtain clear solution, and further condensing the clear solution to obtain extractum; and (3) preparing the liquid medicine by the extractum, flavoring and water, and then obtaining the children cough oral liquid after filtering and condensing the liquid medicine in turn, in particular, in step (2), the purifying means filtering the primary liquid medicine through an ultramicro filter film; and in step (3), the filtering is also carried out by the ultramicro filter film. Through adopting the ultramicro filter film to effectively filter the primary extracted liquid medicine, the preparation technique achieves non-alcoholization production, simplifies processes, shortens production period, and reduces energy consumption and production cost; and at the same time, through adopting a filtering technique of a tubular ultrafilter film to carry out terminal filter for the prepared liquid medicine, the preparation technique ensures the content of effective components, improves clarity of the liquid medicine, improves quality of products, and ensures quality stability of the products.
CN101113146B Process for the separation of blood fat recovery purpose-made monascus active ingredient The invention discloses effective components of Xuezhikang special made Hongqu and separation method thereof. The clinical research of evidence-based medicine proves that: Xuezhikang special made Hongqu can obviously decrease the occurrence rate of coronary heart disease attack and the general death rate. The chemical components of Xuezhikang are researched and ten components are separated from the Xuezhikang and evaluated, and the ten components are: 4-methyl -5(2-methylpropylidene) -1-hydropyrrolidine -2(5-hydro) -acetone (P-3), dehydro-Monacolin K(C-1), stigmast-5, 22-dien-3Beta-ol(C-2), MonacolinK(C-3); 3Beta-hydroxy-5Alpha, 8Beta-cyclodioxy -ergosterin-6, 22-dien-(C-5), N-(1-(tetrahydro-5-oxyfuran-2)-ethyl) acetazoamide(C-6); Daidzein(C-7), glycitein(C-8), genistein(C-9), erythritol (M-1).
US7030164 This invention relates to a highly thermally stable novel anhydrous crystalline polymorphic form of venlafaxine hydrochloride, methods for the preparation thereof, and its use. This invention relates to a highly thermally stable novel anhydrous crystalline polymorphic form of venlafaxine hydrochloride, methods for the preparation thereof, and its use.
WO2012053630A1 Antagonist for mutated androgen receptor [Problem] To provide a novel anticancer drug which is useful for treating prostatic cancer associated with an androgen receptor mutation. [Solution] As the results of intensive studies on mutated androgen-associated diseases for which the conventional anti-androgen drugs are inefficacious, the present inventors found that a compound, said compound being the active ingredient of a medicinal composition according to the present invention, exhibits an effect of inhibiting the transcriptional activation in a human mutated androgen receptor (AR) and has an excellent antitumor effect on a mouse carrying human prostatic cancer cells, thereby completing the present invention. The compound that is the active ingredient of the medicinal composition according to the present invention is useful for treating diseases such as prostatic cancer in which a series of androgen receptors participate.
CN1636576A Application of bioactive glass in preparing medicine for treating gastroduodenal ulcer The present invention relates to the application of bioactive glass in preparing medicine for treating gastroduodenal ulcer, and belongs to the field of biomedicine technology. The present invention features that bioactive glass powder or liquid is filled into soft capsule and is swallowed into stomach and the whole digestive tract to reach the treatment aim. The treating mechanism is that the bioactive glass neutralizes the acid environment to inhibit the depravation of gastroduodenal ulcer caused by gastric acid on one hand and promote soft tissue growth to repair damaged gastric mucous membrane and to heal ulcer on the other hand.
CN102988312A Clopidogrel hydrogen sulfate tablets and preparation method thereof The invention relates to clopidogrel hydrogen sulfate tablets and a preparation method thereof. The preparation is composed of: an active component of clopidogrel hydrogen sulfate, a filling material, a diluent, an adhesive, a disintegrating agent, a lubricant, and a flow aid. The preparation method provided by the invention can satisfy production requirements of tablet industrialization. With the method, medicine quality is controllable. The prepared clopidogrel hydrogen sulfate tablets satisfy quality standard requirements of United States Pharmacopoeia USP 32 version. The stability of the medicine is ensured, and the medicine can be stored for more than 2 years under room temperature.
CN102225207A Dehydrocholic acid-molybdenum heteropoly salt-dehydrocholic acid compound and synthesis method thereof The invention relates to a dehydrocholic acid-molybdenum heteropoly salt-dehydrocholic acid compound. The invention is characterized in that the molecular formula of the dehydrocholic acid-molybdenum heteropoly salt-dehydrocholic acid compound is (C24H33O4)2 [(C4H9)4N] 3(MnMo6O18) [(OCH2)3CNH]2. nH2O, wherein n is 1-4; and the dehydrocholic acid-molybdenum heteropoly salt-dehydrocholic acid compound is synthesizd by the step of performing heteropoly salt organic modification on dehydrocholic acid and molybdenum heteropoly acid in an Anderson structure used as starting materials under the connection effect of covalent bonds. The synthesis method has simple process, is easy to operate and has moderate conditions; the purity of the product is high, and the yield can reach 81%; industrial production, popularization and application can be conveniently realized, and the prepared dehydrocholic acid-molybdenum heteropoly salt-dehydrocholic acid compound has potential important practical value in the fields of medicine, biology and catalysis.
US7282481 Improved thermostability, acid resistance, alkali resistance, resistance to proteolytic enzymes, and DNA synthesis promoting activity A heparin-binding protein functionalized by covalently bonding thereto a sugar chain, a method for producing the protein and a pharmaceutical composition containing the protein as an active ingredient, as well as a method of functionalizing a natural protein having no sugar chain by covalently bonding thereto a sugar chain.
EP2338524A1 Combined gene therapy for the treatment of macroscopic gliomas The present invention relates to vectors expressing Flt3L and TK for use, as a combination therapy, in the treatment of cancer in a mammal that also receives a therapeutically effective quantity of an orally administered nucleoside analogue. The cancer may be a cancer of the brain. The invention also concerns kits comprising such vectors that may be used for treating cancer in mammals.
US20110053922 Spiro (Piperidine-4,2'-Pyrrolidine)-1-(3,5-Trifluoromethyl Phenyl) Methylcarboxamides As NK1 Tachikynin Receptor Antagonists Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R is hydrogen or C1-4 alkyl; R1 is hydrogen, C1-4 alkyl, C(O)OH, C(O)NH2 or (C1-4 alkylene)R10; R2 and R3 are independently hydrogen, C1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C1-4 alkyl, C1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C1-4 alkylene) R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 or C(O)OH; n is 0, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.
US20110027185 Methods of Screening for Anti-Angiogenic Compounds The present invention relates to methods of screening for agents that bind to FBP21. In particular the present invention provides a method of identifying anti-angiogenic agents by screening for agents which are able to bind to FBP21. Compounds identified using the methods and screens of the present invention are useful in the prevention and treatment of conditions associated with angiogenesis.
WO2007026215A1 Pyrazole derivatives as cannabinoid receptor ligands, pharmaceutical compositions containing? them, and processes for their preparation The present invention relates to cannabinoid receptor modulators of general formulas (I) and (II) prodrugs thereof, pharmaceutically acceptable salts thereof, and hydrates and solvates thereof, wherein the meaning of the substituents is as recited in the claims.
EP1032406B1 Reducing blood cholesterol by in vivo precipitation of bile constituents with group ii or -iii metal substances The present invention concerns the use of a substance which causes the precipitation of a bile constituent in the manufacture of amedicament for reducing body cholesterol levels together with methods of manufacture of medicaments comprising same and methods of reducing body cholesterol levels using same.
WO2010118458A1 A multidose package, course and method of treatment for delivering predetermined multiple doses of a pharmaceutical The invention provides: a multidose package containing an imiquimod formulation suitable for treating topical conditions such as actinic keratosis, superficial basal cell carcinoma and external genital warts, said package comprising: a) a dispensing aperture for dispensing the formulation from the package; b) a reservoir containing a sufficient amount of said formulation to provide two or more doses; c) a metered dosage means for measuring a predetermined dose of said formulation, said means comprising an inlet from said reservoir and an outlet to said dispensing aperture; and d) an actuating means for operating said dosage means such that the predetermined dose is delivered to said dispensing aperture; wherein said dose is dispensed without microbial or other contamination or degradation of the formulation in reservoir; a course of treatment of actinic keratosis, superficial basal cell carcinoma or external genital warts comprising provision of a multidose package containing an imiquimod formulation' suitable for said treatment; a method of treatment of actinic keratosis, superficial basal cell carcinoma or external to genital warts with multiple doses of an imiquimod formulation characterised in that the multiple doses are provided by a multidose package; and a method of providing a multidose package containing an imiquimod formulation suitable for treating topical conditions such as actinic keratosis, superficial basal cell carcinoma and external genital warts.
CN101019871A Emerine salicylate oral liquid and its prepn The present invention discloses one kind of emerine salicylate oral liquid prepared with emerine salicylate, sodium pyrosulfite, citric acid, ethyl hydroxyl benzoate, disodium edentate, etc. Of the emerine salicylate oral liquid, emerine salicylate is atropine antagonist to inhibit central AChE activity and maintain relevant skeletal muscle contractility, citric acid is used to regulate pH to 4.8-5.6, and sodium pyrosulfite and disodium edentate are added to avoid the oxidation and hydrolysis of emerine salicylate. Compared with similar medicine, the emerine salicylate oral liquid of the present invention has the advantages of determined curative effect, less side effect and low cost, and is used in treating bulbar patalysis, cerebrellar ataxia, etc.
CN102089314A Macrocyclic indole derivatives useful as hepatitis c virus inhibitors Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1, R2, R4, R5, R6 and R7 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
WO2007040188A1 Medicinal composition for inhibiting the excessive formation of goblet cells It is intended to provide a medicinal composition for inhibiting the excessive formation of goblet cells. As a means of achieving this object, a medicinal composition containing loxoprofen is provided.
US20070269373 benz[e]indole derivatives that absorb and fluoresce in the visible region of light, particularly useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo. Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
WO2011061754A1 A novel 3-substituted 7-imino-2-thioxo-3, 7-dihydro-2h-thiazolo [4,5-di pyrimidin-6-yl - and process for preparation thereof The present invention relates to novel 3-substituted (7-imino-2-thioxo-3, 7-dihydro-2H-thiazolo [4,5-d] pyrimidin-6-yl of formula 1 wherein R is selected from a group consisting of hydrogen, alkyl having carbon no up to 10, allyl, cycloalkyl, aromatic, substituted aromatics (halogen, OH, COOH, OCH3, alkyl, etc), pyridyl, piperidine, piprazine, morphine. R1 is selected from a group consisting of NH2, NHR, N(R) 2(wherein R could be aliphatic or olefinic group up to 10 carbon), hetrocycles such as furan, thiophene, pyrole, prydyl, piprazine, morphine and R2 is O and S separately. Particularly the present invention relates to (7-Imino-3-substituated -2-thioxo-3,7-dihydro-2H-thiazolo[4,5- d]pyrimidin-6-yl)-urea( 15-21) and Furan-2-carboxylic acid (7-imino-3 -substituted -2-thioxo-3,7- dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl)-amide. The compounds of present invention are useful in the treatment of central nervous disorders including, Parkinson disease, Huntington's disease, attention disorder, cognition, Alzheimer disease, depression and hypertension.
WO2013191965A1 Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment cancer and autoimmune diseases Oral pharmaceutical formulations comprising reversible covalent compounds having a Michael acceptor moiety, a process of their production, and use of these formulations for the treatment of diseases treatable by such compounds such as cancer and autoimmune diseases.
CN1939274A Oral preparation containing mediromycin and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains midecamycin. Its preparing process is also disclosed.
CN102028699A Compound pefloxacin mesylate injection and preparation method thereof The invention discloses a compound pefloxacin mesylate injection. The injection consists of the following components in part by weight: 20 to 100 parts of pefloxacin mesylate, 1 to 40 parts of gentamicin sulfate-micronomicin, 1 to 10 parts of raceanisodamine hydrochloride and 800 to 1,000 parts of injection water. The injection is a compound preparation consisting of the pefloxacin mesylate, the gentamicin sulfate-micronomicin and the raceanisodamine hydrochloride, is effective to bacterial diarrhea of dogs, foxes and raccoons, addresses both the symptoms and root causes and alleviates the stress response of an ill animal body. Experiments show that the combined use of the pefloxacin mesylate, the gentamicin sulfate-micronomicin and the raceanisodamine hydrochloride can enhance the treatment effect. The injection is widely applied clinically, can be widely applied to the treatment of bacterial gastrointestinal tracts of the dogs, the foxes and the raccoons, increases the survival rate of the dogs, the foxes and the raccoons and increases the weight of the dogs, the foxes and the raccoons.
US20090053295 Regulatable fusion promoters Fusion promoters are described that combine a RNA polymerase III basal promoter and regulatory elements from RNA polymerase II regulatory regions, and which provide specific regulation of expression from the promoter. Such fusion promoters are useful, for example, for expressing RNAi agents in vivo.
US7763600 Nitric ester derivatives of hormones such as progesterone, used for preventing premature labor, increasing cervical dilatation, in hormone replacement therapy, as hypeortensive agents and for treating dysmenorrhea The invention concerns compounds capable of being fixed on hormone receptors and having a nitrogen monoxide donor group and their use for preventing premature births, increasing cervical dilatation, for use in hormone substitution therapy as anti-hypertensive drug and their therapeutic use for preparing a medicine for use in obstetrics and gynecology.
CA2079814C Cationic lipids for intracellular delivery of biologically active molecules Disclosed are cationic lipids capable of facilitating transport of biologically active agents into cells, including the transfection of cells by therapeutic polynucleotides, the delivery of antiviral drugs, and the introduction of immunogenic peptides. The cationic lipids, comprising an ammonium group, have general structure (I). Also disclosed are adducts of these compounds comprising additional cationic sites that enhance the transfective or transport activity. Structure-activity correlations provide for the selection of preferred compounds to be synthesized for this purpose. Compositions disclosed for use of these cationic lipids include formulations for in vitro transfection and pharmaceutical formulations for parenteral and topical administration of therapeutic agents.
US8333987 Nourexin-4 nano-lipid emulsions The present invention provides compositions and methods for identifying, monitoring, and/or treating tissue inflammation caused by diseases or injury. Inflammatory mediators from the Nourin family are provided as diagnostic markers to detect or monitor a disease or injury that results in inflammation. In addition, the Nourin family antagonist, Nourexin-4 is provided as a therapy to treat diseases or injury. Further, cyclocreatine is provided as an inhibitor of Nourin formation, which can be used as a therapy to treat injury and inflammation.
CN1907978A Vibralactone, preparation method and medicinal application thereof The invention discloses an extracting method from ferment liquid of Boreostereum vibrans, which can prevent hyperlipemia, diabetes and adiposis.
CN103340861A Rabeprazole sodium composition for injection The invention provides a rabeprazole sodium composition for injection and relates to o the technical field of medicaments and medicament manufacturing. The main medicaments of the composition are rabeprazole sodium and melatonin, wherein the he melatonin comprises a quick release part and a slow release part contained in cyclodextrin. The rabeprazole sodium composition for injection provided by the invention can be used for improving the treatment effect of the granisetron, avoiding instability, quick distribution and elimination and the like of MT ((Metal Thionein) caused by oral absorption, reducing the first-pass effect of the MT, reducing the dosage of the rabeprazole sodium and lowering the adverse reaction of the rabeprazole sodium. The medicament administration design combining the quick release with the slow release satisfies secretion characteristics of the MT, can be used for solving the problem that the half-life period of the MT is short and increasing the biological utilization.
US20090082426 Dimers of artemisinin derivatives, preparation thereof and therapeutic use thereof The present invention relates to dimers of artemisinin derivatives, to processes for the preparation of such dimers, to methods of treatment comprising administration of such dimers, and to intermediates to such dimers.
CN102860991A Medicine composition containing febuxostat and preparation method thereof The invention relates to a medicine composition containing febuxostat. The medicine composition comprises water-soluble solid dispersing carriers, diluents and lubricants, wherein the proportion of the febuxostat and the water-soluble solid dispersing carriers is 1: (0.5-3) according to parts by weight, and the water-soluble solid dispersing carriers include one or a plurality of polyethylene glycol, povidone and poloxamer. The invention further discloses a preparation method of the medicine composition. The preparation method includes: evenly mixing the febuxostat and the water-soluble dispersing carriers, adding alcohol, dissolving the alcohol in water bath, performing heating to volatilize the alcohol, adding the diluents, evenly stirring, sieving, drying, granulating straightening, and tabletting or capsule filling. The medicine composition containing febuxostat adopts the solid dispersing technology, overcomes the shortcomings of poor febuxostat solubility and low bioavailability, and unexpectedly has good stability. The production process is simple and can be used in industrial production.
US20110306618 JNK Modulators Compounds of formula (I) modulate JNK wherein X1 and X2 are each simultaneously N or CH; X3 is CH—R2 Or N—SO2R, where R is lower alkyl; R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; R2 is (II), where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof.
US7192742 Prepared by culturing Beauveria in medium; substances thus obtained are less toxic, specifically inhibit acyl-Coenzyme A: cholesterol acyltransferase, and inhibit formation of oil droplets in macrophages (Beauveria) sp. FO-6979 (FERM BP-6681), which belongs to the genus Beauveria and is capable of producing FO-6979-M0, -M1, -M2, -M3 and -M4 substances, is cultured in a medium to thereby accumulate the FO-6979-M0, -M1, -M2, -M3 and -M4 substances in the liquid culture medium. Then the FO-6979-M0, -M1, -M2, -M3 and -M4 substances are collected from the culture medium. The substances thus obtained are less toxic, specifically inhibit acyl-Coenzyme A: cholesterol acyltransferase, and inhibit the formation of oil droplets in macrophages. Owing to these characteristics, the above substances are useful in preventing and treating human diseases caused by cholesterol accumulation.
WO2008004127A3 Method for administering tolperisone The present invention is directed to methods of administering tolperisone (2,4'-dimethyl- 3-piperidinoproρiophenone; 1-propanone, 2-methyl-1-(4-methylphenyl)-3-(-piperidinyl)), and kits comprising the same.
CN101053571A Gentiopicroside drop pill and preparation method thereof A gentiopicroside dropping pill contains gentiopicroside and medicinal groundsubstance components with a dosage proportion by weight of 1:0.5-10. The format of the gentiopicroside dropping pills is 5-500mg/grain. The preparation method of the gentiopicroside dropping pills comprises the following steps: refluxing the gentian coarse powder with ethyl hydrate for extracting, combining and concentrating the extract, standing it overnight at low temperature; performing soup centrifugation and filtration; eluting the filtrate with macroporous resin column; collecting the eluent, concentrating it at reduced pressure to concrete shape, vacuum (freeze) drying it to obtain a crude product; refining it to obtain pure gentiopicroside; selecting medicinal groundsubstances for preparing solid dispersion as a carrier and suspending gentiopicroside in the melting carrier, and then working out gentiopicroside dropping pills by adopting the dropping method. The gentiopicroside dropping pills, as gentiopicroside dropping pill dose, possesses remarkable liver-protection and cholagogic functions. Since the medicament is highly dispersed molecularly in the groundsubstance, and the groundsubstance with water-solubility can accelerate dissolution velocity and absorption rate of drugs, then the bioavailability is high.
US20130011482 Dual component medicament delivery system A medicament delivery system is disclosed. The system comprises a descending formulation for delivering the medicament and an ascending formulation to protect a patient being treated with the medicament from the side effects thereof.
CN1843339A Use of resveratrol in treating rheumatoid arthritis and non-inflammatory disease The invention relates to an application of resveratrol in drug treating atrophic arthritis and non-infectious inflammation. The usage method is that: oral 20 mg/kg, three months as a course of treatment and for 2-3 curses; and 10mg/kg, one month as a course of treatment and for 1-2 courses. The effect is better than leflunomide, ledertrexate, and pavlin when resveratrol is used to treat atrophic arthritis; and the effect is better than acetophen when it is used to treat non-infectious inflammation.
EP0914435B1 Hybrid interferon compositions and methods of use The present invention describes hybrid interferon fusion polypeptides formed of a first segment that contains the N-terminal amino acid sequence of an interferon-tau polypeptide, and a second segment that contains the C-terminal amino acid sequence of a non-tau interferon type I polypeptide. The two segments are joined in the region of a mature interferon polypeptide between about residues 8 and 37. Also described are nucleic acid sequences encoding such interferon fusion polypeptides, expression vectors containing such sequences, and therapeutic applications of the interferon fusion polypeptides. The therapeutic applications include antiviral and anticellular proliferation applications. One advantage of the interferon fusion polypeptides of the present invention is that they do not have cytotoxic side-effects when used to treat cells.
WO2011005759A2 Lonidamine analogues for fertility management Fertility management can include: administering to the subject one or more doses of a compound according to Formula I so as to reduce fertility in the subject. Fertility management can also include administering an effective amount of the compound to: impair Sertoli cell function in a male subject; inhibit spermatogenesis in the subject; reduce testis weight in the subject; reduce ovary weight in a female subject; reduce serum progesterone in the female subject; impair ovarian follicle function in the female subject; causing reversible fertility in the subject. In order to return fertility, the method can include ceasing administration of the compound to the subject so as to return fertility in the subject. The compound can be administered for irreversibly sterilizing the subject.
US20070264195 Modulation of Activity of Neurotrophins The present invention relates to methods for modulating the activity of one or more neurotrophins, such as neural growth factor (NGF), brain derived neurotrophic factor (BDNF), neurotrophin-3, and neurotrophin-4 (NT-4), in an animal and methods for treatment of a disease or disorder in an individual by modulation of neurotrophin activity. The modulation is carried out by interfering with binding between a neurotrophin and a receptor of the Vps10p-domain receptor family or modulating the expression of a receptor of the Vps10p-domain receptor family. Methods for screening for agents capable of modulating neurotrophin activity and agents selected using these screening methods are also disclosed, as are methods for determining the effect of an agent on one or more neurotrophins in cells. The present invention also pertains to methods for modulating the transport of one or more neurotrophins.
EP1402886B1 Lipolysis accelerator for reducing body weight and medicinal use A lipolysis accelerator which has no peculiar scent or flavor, has excellent general-purpose properties, is effective in improving an obese constitution by accelerating adipose tissue diminution in the whole or a local part of the body or in inhibiting or preventing obesity by preventing adipose tissue increase. The lipolysis accelerator contains as the active ingredient a compound represented by the following formula (I) wherein Z represents the group represented by the following formula (II) or (III), and R<1> and R<2> each is hydrogen or a glucose residue, provided that at least either of R<1> and R<2> is hydrogen.
US7138410 Aza-bicyclic N-biarylamides with affinity for the α7 nicotinic acetylcholine receptor The invention relates to novel 1-aza-bicyclic N-biarylamides, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning ability and memory.
CN101773539A Prescription with function for mitigating and curing osteoarthrosis The invention discloses a prescription with function for mitigating and curing osteoarthrosis, which comprises the components by weight percent: 3.3-66.7% of glucosamine hydrochloride, 10.67-16% of chondroitin sulfuric acid, 4-9.33% of soybean extract, 2.67-5.33% of pseudo-ginseng extract, 4-13.33% of drynaria rhizome extract, 1.33-4% of antioxygen, 1-3% of lubricating agent A and 0.267-0.533% of lubricating agent B. The preparation method of the prescription comprises the steps of: jointly mixing, filling capsule, polishing, detecting semi-manufactured goods and packing into capsule dosage. With the clinical observation of Shanghai No.6 People's Hospital, the prescription has high ramollescence for osteophyte or bony spur, has various coordinated effects of analgesia, anti-inflammation, detumescence and microcirculation improvement, and the like, and has effective rate of 86.67% for curing osteoarthrosis.
US20100050281 Identification of Genes and Their Products Which Promote Hybrid Vigour or Hybrid Debility and Uses Thereof The present invention relates to a method of identifying candidate genes and the proteins encoded by them that are useful in the inducement of hybrid vigour, hybrid debility and/or the diagnosis, prognosis and treatment of disease. In particular, the present invention relates to a method for identifying candidate genes capable of producing hybrid vigour or hybrid debility in an animal or plant, comprising the steps of: (i) comparing the mRNA sequence of alleles of candidate genes isolated from an animal or plant which exhibits hybrid vigour or hybrid debility with the nucleotide sequences from the corresponding alleles isolated from the parents of said animal or plant; (ii) identifying mRNA sequence differences in the alleles from said animal or plant which exhibits hybrid vigour or hybrid debility which codes for amino acid sequence variation; and (iii) identifying that the amino acid sequence variation between alleles of the candidate gene in said animal or plant is encoded by mRNA sequences which are located within two or more different exons within the candidate gene.
CN102643214A Preparation method and preparation of vorinostat I crystal form large grains The invention provides a preparation method of vorinostat I crystal form large grains as a medicament for treating cutaneous T cell lymphoma and a preparation prepared from vorinostat obtained by the preparation method. The preparation method can crystallize in place once, is simple, effective and suitable for large-scale industrial production and further has greater commercial application value. The obtained preparation is good in dissolution effect.
CA2601808C Use of macelignan for treatment of brain diseases The present invention relates to the novel use of lignan compounds. More particularly, the present invention relates to a pharmaceutical composition for treating or preventing a brain disease, comprising a lignan compound such as macelignan or a Myristica fragrans extract as an active ingredient, as well as the method and use for treating or preventing a brain disease using the lignan compound. The lignan compound has the effects of antioxidation, brain cell protection and anti inflammation. Accordingly, said lignan compound will be highly useful for treating or preventing a brain disease.
CN101716153A Ornidazole ester microsphere solid preparation The invention discloses an ornidazole ester microsphere solid preparation. Specifically, ornidazole ester microspheres are prepared by adopting film dispersion technology through the combination of hydrogenated yolk lecithin, cholesterol, poloxamer 188, sodium glycyl-cholate and ornidazole serving as active component with certain contents, and then the ornidazole ester microspheres are mixed with certain accessories to obtain the solid preparation such as tablets and capsules. The solid preparation has the surprising technical effects of high dissolution degree, high bioavailability, small toxic and side effect and the like.
EP2548877A1 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors The present invention provides 6-5 membered fused pyridine ring compounds according to Formula I or pharmaceutically acceptable salts thereof. or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
CN102548555A Compositions and methods for treating parkinson's disease This application describes compositions of receptor inhibitors, including typical antipsychotic agents, for example haloperidol, and methods of use for treating clinical signs or symptoms of Parkinson's disease. Furthermore, this application describes compositions and methods to induce supersensitivity in dopamine D2 and other receptors involved in Parkinson's disease as a means of alleviating the clinical signs or symptoms of Parkinson's disease.
WO2011121308A1 New polymorph The invention provides a new polymorph of 1-(2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl)benzylcarbamoyl)-L-proline-N,N-dimethylamide, pharmaceutical compositions containing it and its use in therapy.
US20100076074 Carbamate reducers of skeletal muscle tension The present invention relates to new carbamate skeletal muscle relaxants, pharmaceutical compositions thereof, and methods of use thereof.
CN101502529B Application of vincetoxicoside B in preparing antidiabetic medicament The invention discloses the application of vincetoxicoside B in the preparation of anti-diabetic drugs. The invention provides a novel choice and idea for the existing anti-diabetic drugs, widens the selecting field of the anti-diabetic drugs and contributes to the development of the technical field; the applied vincetoxicoside B of the invention is proved to have remarkable anti-diabetic effect;and the invention is selected from the extract of natural drugs having specific chemical structure, therefore, the feeding is quantifiable in the preparation and the invention is applicable to the preparation of drugs in modern forms.
US6960600 a triazole or amidazole compound containing oxy, hydroxy or aromatic rings; active on candidoses, cryptococcoses caused by Candida albicans; prevention of mycosic diseases in individuals with immunodeficiency. The invention concerns novel azole or triazole derivatives of formula (I), wherein: X, Ar1, Ar3, A, R1, R5, R6, R7 and B are such as defined in the description, their preparation method and their use as antifungal medicines.
EP1332155B1 Immunization of dairy cattle with gapc protein against streptococcus infection The GapC plasmin binding protein genes of Streptococcus dysgalactiae (S. dysgalactiae), Streptococcus agalactiae (S. agalactiae), Streptococcus uberis (S. uberis), Streptococcus parauberis (S. parauberis), and Streptococcus iniae (S.iniae) are described, as well as the recombinant production of the GapC proteins therefrom. Also described is the use of the GapC proteins from those species in vaccine compositions to prevent or treat bacterial infections in general, and mastitis in particular.
CN102755648A Preparation method of anti-aging human universal nutritional supplement An anti-aging human universal nutritional supplement is a latest product which is invented at present, is capable of resisting aging, remaining youth and enabling people to be health and longevial and integrates medical care. The product is prepared by various vitamins, amino acid, mineral substances, allicin, probiotics and other 42 components. Before the invention, an antioxidant vitamin mineral supplement is invented by Americans. The product can play a large role in reducing the risks of various chronic diseases. Compared with the former product, the product contains various nutritional components, and the former product contains 12 nutritional components, and the latter product contains 42 nutritional components. In function, the risks of some chronic diseases can be reduced by the former product, and the latter product has more functions and can supplement various human nutritional components, resist the aging, clear the damage of free radicals to human cells, remain youth, resist the aging, prevent and treat the diseases and enable the people to be health and longevial.
EP2771341A1 Novel compositions and methods for treating cancer Provided herein are methods and compositions inter alia for treating diseases, including hyperproliferative diseases, migraine headaches, and depression.
US20090099250 Benzocycloheptene derivatives as estrogens having selective activity The present invention describes non-steroidal compounds of the general formula (I) in which A is in which X1 means one or more groups on the phenyl ring and represents independently of one another a halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C3-C6)cycloalkyl-O, (C1-C14)acyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro(C1-C4)alkyl radical, —CHO or CN, and X2 means one or more groups on the phenyl ring and represents independently of one another an H, halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro-(C1-C4)alkyl radical, —CHO or CN, as Estrogens.
WO2013142326A1 5-carbonylamino-/(sulfonamido-) substituted benz imidazoles and use thereof treatment of tuberculosis The present invention discloses novel 5-/6- or 5-/7- substituded benzimidazoles and pharmaceutically acceptable salts thereof. Another aspect of the invention relates to their use in treating a patient infected by Mycobacterium tuberculosis or Francisella tularensis.
EP1214084B1 An anti-oxidant preparation based on plant extracts for the treatment of circulation and adiposity problems A preparation based on plant extracts, with an anti-oxidant action which is particularly useful in the prevention and treatment of circulation problems and in the prevention and treatment of surplus fat deposits, characterised in that its active ingredients comprise, in association, Ginkgo bilobabiflavones, catechine and/or epicatechine, iodine and a component selected from among madecassic acid, asiatic acid, asiaticoside or combinations thereof.
US20120328708 Disinfectant composition and its use in dental treatment The present invention concerns a disinfectant or antimicrobial composition for use in dental treatment, such as treatment and/or prevention of periodontitis, gingivitis or other forms of oral infection. The present Inventor found that microorganisms that infect the dental tissues and cause inflammation thereof, are susceptible to osmotic stress, to such extent that the application of a hypertonic composition is effective in curing or preventing infection and/or inflammations. It was furthermore found that these microorganisms are also susceptible to acidic stress. The present invention therefore provides compositions that induce osmotic stress in microorganisms causing infection of dental tissue when topically applied thereto, preferably osmotic as well as acidic stress. The present invention also concerns the methods and uses involving the compositions of the invention.
CN102068471A Externally applied medicine for treating carbuncle diseases The invention relates to the technical field of medicines, and provides an externally applied medicine for treating carbuncle diseases, which is prepared by mixing and crushing the following raw materials uniformly in part by weight: 10 to 20 parts of dried alum, 10 to 20 parts of borax, 0.5 to 3 parts of calamine, 5 to 10 parts of cotton rose, 0.5 to 2 parts of white snail and 5 to 8 parts of camphor. The externally applied medicine for treating the carbuncle diseases has a novel, advanced and unique formula of the raw materials, has simple and convenient processing technology, a simple using method, a quick curative effect and high cure rate, and does not have toxic or side effects.
US20120329803 Dihydropteridinones, method for production and use thereof The present invention relates to new dihydropteridinones of general formula (12) wherein the groups R1 to R5 and L, n, and m have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.
CN101152164B Anti-cicatrix externally used pad pasting containing anti-hypertrophy cell medicament and method for preparing the same The invention discloses an anti-cicatricial topical drug film containing anti-mast cell medicine and the preparation method. The anti-cicatricial topical drug film contains silica gel drug film, which is added with anti-mast cell medicine. The anti-cicatricial topical drug film of the invention is capable of effectively curing scar. After the drug combination in the drug film is screened and the drug combination is optimized, the anti-cicatricial topical drug film does not change the hormone levels of patients. Thereby, the invention is not only fit for curing scars of common population and children, but also capable of curing wounds except severe infection. Besides, the product improves the treating effect of gel scar drug film and widens the scope of treating population. The anti-cicatricial topical drug film of the invention is characterized by simple preparation process and low cost.
WO2006091450A1 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds Substituted 4-piperidin-l -yl-7H-pyrrolo[2,3-D]pyrirnidine compounds are disclosed, as well as compositions comprising them and methods of their use for the treatment, prevention and management of various diseases and disorders.
CN101797264B Amphotericin B lipid complex for injection and preparation method thereof The invention discloses an amphotericin B lipid complex for injection, comprising amphotericin B, cholesterol sulfate and phospholipids with the molar ratio of 1:0.5-10:0.3-10. The invention also discloses a preparation method of the amphotericin B lipid complex for injection. In the amphotericin B lipid complex for injection, the complexing ratio is more than or equal to 95 percent, the particlesize is less, the average particle size is less than or equal to 100nm, and the particle size after redissolving is 50-250nm. The amphotericin B lipid complex for injection is stable in physiologicalsaline and blood plasma, thus having lower toxicity and infusion reaction; the amphotericin B lipid complex for injection can be diluted by adopting the physiological saline, thus further improving the range and convenience of clinical use; and the preparation method of the amphotericin B lipid complex for injection has simple preparation method and technique and is convenient for large-scale production.
CN101773516A Acidic buffer gel preparation for vaginas and preparation method and application thereof The invention discloses an acidic buffer gel preparation for vaginas, which takes polycarbophil and carbomer as acid agents, sodium salts of methyl hydroxybenzoate, hydroxyphenyl ethylester and propyl hydroxybenzoate as alkaline agents, and water and glycerol as solvents to form a ph buffer system with buffering capacity. The invention also discloses a preparation method of the preparation. The preparation process does not need strong acid or strong alkali to adjust the pH value, i.e., the ph value of an intermediate does not need to be frequently detected, so that the pH value of the prepared acidic gel preparation is accurately between 3. 5 and 3.1, and is very close to the lower limit of the pH value of the physiological vagina, and one-time use can maintain the effect for not less than 3 days.
US7547682 Useful as a candidate for a vaccine against ticks, particularly Ornithodoros moubata, tick-borne infections such as rickettsiosis, filariasis, Q fever, African recurrent fever, or viral encephalitis A novel galectin, a polynucleotide encoding the same, a vector and a transformant comprising the polynucleotide, an antibody against the galectin, and a screening method for screening a substance capable of modifying the galectin, are disclosed. According to the galectin, polynucleotide, or vector, it is possible, for example, to exterminate ticks, or to treat or prevent tick-borne infections such as rickettsiosis, filariasis, Q fever, African recurrent fever, or viral encephalitis.
EP1519754A1 Use of cetp inhibitors and optionally hmg coa reductase inhibitors and/or antihypertensive agents This invention relates to cholesterol ester transfer protein (CETP) inhibitors, pharmaceutical compositions containing such inhibitors, and the use of such inhibitors to treat certain disease/conditions optionally in combination with certain therapeutic agents e.g., antihypertensive agents.
US20100105689 Novel 1,4- and 1,5-diarylsubstituted 1,2,3-triazoles useful as potassium channel modulators This invention relates to novel 1,4- and 1,5-diarylsubstituted 1,2,3-triazole derivatives that are found to be potent modulators of potassium channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of potassium channels.
WO2014160181A1 Pyrazole compounds, compositions and methods for treatment of degenerative diseases and disorders Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
EP2508180A1 Sn-1(3) Monoacylglycerides and lipid absorption The present invention relates generally to the field of lipids and in particular aims at improving lipid absorption, for example under conditions of lipid maldigestion or malabsorption. One embodiment of the present invention relates to a composition comprising sn-1(3) monoacylglycerols, wherein the sn-1 or sn-3 position is occupied by an acyl group such as a fatty acid and the sn-2 position remains unoccupied. The fatty acid may be one with anti-inflammatory properties.
WO2009118338A2 Use of a polyphenolic type compound for preventing or treating a polyglutamine expansion neurodegenerative disease The present invention relates to the use of polyphenolic type compounds as disclosed in the specification for preventing or treating a polyglutamine expansion neurodegenerative disease.
CN101780282A Chitosan-carrying mitomycin nano targeting preparation and preparation method thereof The invention discloses a chitosan-carrying mitomycin nano targeting preparation and a preparation method thereof, which relate to a medicine-carrying chitosan nano particle. The invention provides a chitosan-carrying mitomycin nano targeting preparation and a preparation method thereof. The chitosan-carrying mitomycin nano targeting preparation comprises chitosan nano particles for connecting mitomycin, which are dispersed in water. The mass ratio of mitomycin to nano particles is 1:(2-10), and the concentration of the nano particles in water is 1-20 mg/ml. The method comprises the following steps: preparing the chitosan nano particles; preparing folic acid modified nano particles; preparing PEG modified nano particles; preparing mitomycin ester succinate; and adding the mitomycin ester succinate and the chitosan nano particles into different modified nano particles, adding 1-[3-(Dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride, obtaining the mitomycin-carried nano particles after reaction, and dialyzing to remove the unreacted mitomycin and other byproducts, thereby obtaining the chitosan-carrying mitomycin nano targeting preparation.
WO2006041135A1 STAT3 PHOSPHORYLATION INHIBITOR AND Notch1 EXPRESSION INHIBITOR A STAT3 phosphorylation inhibitor and Notch1 expression inhibitor each comprising as an active ingredient a compound of the formula: (1) wherein each of R1, R2 and R3 is a hydrogen atom or a methyl group, and X is a C10-C28 linear or branched alkyl, alkylene or alkenylene group.
WO2013157034A1 Composition for preparing external skin preparation [Problem] To provide a composition for preparing an external skin preparation with which an external skin preparation, capable of limiting dripping and of causing carbon dioxide gas to be absorbed more uniformly than in the past and which is easy to remove after use, can be prepared. [Solution] A composition for preparing a foaming external skin preparation that causes generated carbon dioxide gas to be absorbed percutaneously, wherein: the composition is provided with a first agent, which is a gelled aqueous composition containing sodium stearoxy PG-hydroxyethyl cellulose sulfonate, stearoxy hydroxypropyl methylcellulose and a carbonate salt, and a granular second agent containing an acidic substance that acts as an acid with respect to the carbonate salt and generates carbon dioxide; and the proportions of the various components with respect to the first agent are 0.5 - 2 mass% sodium stearoxy PG-hydroxyethyl cellulose sulfonate, 0.5 - 2 mass% stearoxy hydroxypropyl methylcellulose, and 0.5 - 5 mass% carbonate salt.
US7186687 for topical administration of peptide copper complex with corticosteroids, coal tar, anthralin, calcipotriene, and tazarotene; dermatology; cosmetics A method for treating psoriasis of the skin of a patient employs topically applying to the affected skin a composition comprising at least one peptide copper complex. In other embodiments, the present invention is directed to such a method where the composition used therefor further comprises certain disclosed active agents, including active drug and active cosmetic substances. In a related aspect, further embodiments of the present invention are directed to compositions comprising at least one peptide copper complex and certain active drug and active cosmetic substances that render the compositions particularly effective in treating psoriasis.
CN103340978A Chinese and western combination drug for treating frequent micturition and urgent urination The invention provides a Chinese and western combination drug for treating frequent micturition and urgent urination. The Chinese and western combination drug is formed by combining the following medicinal materials in parts by weight: 15 parts of achyranthes bidentata, 15 parts of herba pyrrosiae, 20 parts of christina loosestrife herb, 10 parts of cistanche, 15 parts of radix rehmanniae preparata, 0.2 part of azithromycin tablets and 0.2 part of ofloxacin hydrochloride. The Chinese and western combination drug for treating frequent micturition and urgent urination is obvious and quick in treatment effect and lasting in efficacy.
CN102949343A Method for increasing fat-soluble drug loading capacity in liposome The invention discloses a preparation method of liposome for increasing fat-soluble drug loading capacity, which comprises the following steps: dissolving fat-soluble drugs in an organic solvent, mixing with a water phase to obtain an emulsion, performing high-pressure homogenization to obtain liposome with a uniform particle size, and finally performing rotary evaporation, concentration, and freeze drying to obtain the liposome with high drug loading capacity. The method can not only obtain high encapsulation efficiency, but also improve curative effect and reduce toxicity of drugs.
CN101856332A Method for preparing 8, 9-single-epoxy brevifolin PLGA microspheres The invention discloses a method for preparing 8, 9-single-epoxy brevifolin PLGA microspheres, which comprises the following steps of: adding PLGA into CH2Cl2 to obtain PLGA solution, dissolving 8, 9-single-epoxy brevifolin into PBS to obtain medicinal solution, precisely measuring a certain amount of medicinal solution and adding the medicinal solution into a proper amount of PLGA solution, ultrasonically emulsifying the solution to obtain foremilk, adding the foremilk into PVA aqueous solution, stirring the solution by a magnetic stirrer, evaporating the CH2Cl2, and solidifying microspheres to obtain the 8, 9-single-epoxy brevifolin PLGA microspheres. The 8, 9-single-epoxy brevifolin PLGA microspheres prepared according to the preparation method of the invention can increase the dissolubility and stability of the 8, 9-single-epoxy brevifolin, and more important, has targeting property so as to reduce the dose, reduce the toxic or side effect and improve the bioavailability.
US20090123569 Coverage indicating technology for skin sealants using tannates A composition having various color changing tannates may be used to indicate that the composition has dried. The tannates change color in contact with an acid. The composition may be, for example, a skin prep, skin sealant, food product, paint or other building material or other product that undergoes a phase change. The tannate may be added either directly to the composition, incorporated into a sponge on an applicator through which the composition is dispensed and applied, applied separately or applied simultaneously from a separate reservoir. The amount of tannate in the composition can be adjusted to provide a visual cue to the user of the application area and the extent of cure.
WO2014101865A1 Composition of glucose derivative and proline, crystal, preparation method and application Disclosed are a composition of glucose derivative and proline, a crystal, a preparation method, and an application. In an X-ray powder diffraction diagram of an eutectic crystal, when the diffraction angle is 2θ, characteristic diffraction peaks comprise 4.339, 11.499, 12.835, 13.921, 15.294, 16.212, 16.804, 17.154, 18.335, 19.274, 19.982, 22.710, 23.218, 24.885, 27.940, 29.612, and 30.313, and the 2θ error range is ±0.1. The method comprises: mixing a compound A solution with an L-proline solution, and performing cooling and crystallization. The present invention further provides an application of the crystal in medicine preparation. The eutectic crystal in the present invention features high water-solubility, low hygroscopicity and high stability, and is suitable for manufacturing a variety of preparations.
WO2007062797A1 Amino-substituted azo-heterocyclic compounds for treating inflammatory conditions Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein X1 is -S-, -O-, -N=N-. -NR5-, -CR5=CR6-, -CR5=N-, wherein R5 and R6 are independently hydrogen or C1-C3 alkyl; R1 is hydrogen or C1-C3 alkyl or cyclopropyl; R2 is an optionally substituted phenyl or 5- or 6-membered monocyclic heteroaryl ring; R3 is an optionally substituted carbocyclic ring of 3 to 7 ring atoms, or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; R4 is a group other than hydrogen, methyl or ethyl of formula Q-[Alk1]m-[X]n-[Alk2]p-[Z}s- wherein m, n p, and s are independently 0 or 1 ; Q is hydrogen or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; Alk1 and Alk2 are independently optionally substituted C1-C3 alkylene radicals; X is -O-, -S-, -C(=O)-, - S(=O)-, -S(=O)2-, -CH(R7)-, -N(R7)-, or, in either orientation -SO2N(R7)- or - C(=O)N(R7)-, wherein R7 is hydrogen, or R7 represents a C2-C4 bridge between the C or N atom of X to which it is attached and a carbon atom of Alk2 and Z is -CH2, - C(=O) or -S(=O)2.
EP1009387B1 Stabilized sustained release tramadol formulations A stabilized sustained release oral solid dosage form which includes an effective amount of tramadol or a pharmaceutically acceptable salt thereof dispersed in a matrix of a hydrophobic material comprising a wax-like substance which was melted or softened during the preparation of the matrix, is cured at a temperature from about 35 °C to about 65 °C for a time period from about 4 to about 72 hours, such that the formulation, when subjected to in vitro dissolution after exposure to accelerated storage conditions of at least one month at 40 °C/75 % RH, releases an amount of tramadol which does not vary at any given dissolution time point by more than about 20 % of the total amount of tramadol released when compared to in vitro dissolution conducted prior to subjecting the dosage form to the accelerated storage conditions.
CN102443005A Spiroheterocycle compound of chalcone and application of spiroheterocycle compound The invention relates to a spiroheterocycle compound with a general formula (I), stereoisomers, enantiomer, tautomers or mixtures thereof, or pharmaceutically acceptable salts, solvates or predrugs thereof, wherein II, R1, R2, R3, Ar1 and Ar2 are as defined herein. The compound provided by the invention has a better application prospect in the medicine aspect, and the application prospect specifically comprises but is not limited to preparation of anti-tumor medicines, tyrosine kinase inhibitor medicines, medicines for treating diseases caused by oxidative stress and anti-inflammation medicines for treating inflammation-related diseases.
US20110207704 Novel Oxadiazole Compounds Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed.
CN1562992A Technique for extracting general coumarin and monomer components from cnidium fruit and medicinal preparation In this invention process, fructus cnidii is used as raw material is extracted, by carbon dioxide supercritical extraction, to obtain total coumarin, with effective content being more than 50%. Cnidiadin monomer is separated from extract. Said invention total coumarin is used as main active ingredient, adding (or not) pharmaceutical excipient or ingredient having synergistic action, to produce clinical pharmaceutical prepns.
CN102108081A Novel crystal form of Iloperidone and preparation method thereof The invention relates to a novel crystal form of antischizophrenic medicament Iloperidone and a preparation method thereof. The Iloperidone is an antischizophrenic medicament, and the chemical name of the Iloperidone is 1-[4-[3-[4-(6-fluorine-1,2-benzisoxazole-3-yl)-1-piperidyl]-propoxy]-3-methoxyphenyl]ethyl ketone. The novel crystal form provided by the invention has the characteristics of high purity and good stability.
US20090149448 Phenoxyacetic Acid Derivatives Useful for Treating Respiratory Diseases The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
US7037523 Controlled release compositions for macrolide antimicrobial agents The present invention provides a controlled release pharmaceutical composition of an acid labile, poorly soluble drug having pH dependent solubility profile in aqueous environment. In a preferred embodiment the drug is combined with a practically water insoluble polymer an optimizing agent and optional additives to produce a controlled release of therapeutic agent when compositions is exposed to aqueous environment.
WO2006031191A1 Compositions comprising compounds capable of forming a reversible bond or association with gaseous nitric oxide The invention relates to compositions and methods for use in the delivery of gaseous nitric oxide (NO) to a mammal, preferably a human. The compositions for the delivery of the gaseous NO comprise a compound capable of forming a reversible bond or association to NO. Suitable compounds are among others alcohols, carbohydrates and proteins. The nitric oxide is delivered to a mammal for prophylactic and/or therapeutic purposes.
US20050277656 Combination comprising docetaxel and a CDK inhibitor A first aspect of the invention relates to a combination comprising docetaxel, or a derivative or prodrug thereof, and a CDK inhibitor. A second aspect of the invention relates to a pharmaceutical product comprising docetaxel, or a derivative or prodrug thereof, and a CDK inhibitor as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a docetaxel, or a derivative or prodrug thereof, and a CDK inhibitor to a subject.
WO2010072144A1 Substituted phenylpiperazinyl aralkylalcohol derivatives, pharmaceutical compositions containing such derivatives and uses thereof The substituted phenylpiperazinyl aralkylalcohol derivatives shown as the following formula (I), and the salts and hydrates thereof, in which C1 and C2 are chiral carbon atoms, the compound is one of six isomer of (1RS, 2SR), (1RS, 2RS), (1R,2S), (1S, 2S), (1R, 2R), or (1S, 2R), and R, R1, R2, R3 and Ar are defined as the definition in description, These derivatives are non-opioid analgesics, and they have good analgesic effects and lower toxicity and side effects. The pharmaceutical compositions containing such derivatives and the uses thereof.
CN102988381A Application of Houttuynoid A for preparing medicine for promoting insulin to secrete The invention discloses application of Houttuynoid A for preparing a medicine for promoting insulin to secrete, belonging to the field of pharmacy. The application of Houttuynoid A for preparing the medicine for promoting insulin to secrete is disclosed for the first time; because the skeleton type belongs to a brand new skeleton type and the activity of Houttuynoid A for promoting insulin to secrete is strong unexpectedly, the possibility that other compounds give any inspiration does not exist; Houttuynoid A has outstanding substantive characteristics; and simultaneously, Houttuynoid A has obvious progress for preventing and treating type 2 diabetes mellitus.
US7728005 such as N-(2-bromophenyl)-N'-[2-(4-fluorophenoxy)ethyl]urea, having superior antiinflammatory and analgesic activity The present invention relates to an ether derivative represented by the formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description, and an ether derivative represented by the formula (III), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description; a pharmaceutical composition containing the ether derivative; and a package containing the pharmaceutical composition and a description of use thereof. A pharmaceutical composition of the present invention, which contains this compound of the present invention has a superior anti-inflammatory and analgesic activity and is useful as various pharmaceutical agents such as an anti-inflammatory agent, an analgesic, a therapeutic agent for inflammatory bowel disease, a therapeutic agent for pollakiuria and/or incontinentia, a therapeutic agent for asthma and the like.
WO2008013807A9 A novel lactic acid formulation of mk-0457 useful for the treatment of cancer A lactic acid formulation, and a process to prepare that formulation, of MK-0457 is disclosed:. Such a formulation is useful in the treatment of cancer.
CN103550301A Preparation for treating bromhidrosis The invention discloses a preparation for treating bromhidrosis. The preparation comprises the following components in parts by weight: 1-3 of yellow lead, 10-20 parts of realgar, 3-5 parts of radix angelicae, 4-8 parts of fructus cnidii, 3-8 parts of clove, 4-10 parts of alum, 10-20 parts of vermiculite schist seu and 20-30 parts of talcum powder. Compared with the prior art, the preparation has the beneficial effects that the formula and the technology are simple and reasonable, the using effect is remarkable and durable, and the preparation has good stability, moderate performance, no toxic or side effects and no damage to skin, and is safe and reliable.
WO2014134053A1 Ascorbate esters of omega-3 fatty acids The present invention provides ascorbate esters of omega-3 fatty acids as their pharmaceutically-acceptable salts and pharmaceutically- acceptable formulations for use as dietary supplements with enhanced antioxidant properties, in improving the effectiveness of other drugs and in treatment of hypertriglyceridemia, hypercholestolemia, diabetes, psychiatric and neurological disorders, attention deficit and hyperactivity disorder, and as cosmeceuticals.
US20120189685 Wound dressing comprising an anti-inflammatory pain-killing agent and a complex of silver ion and a transitional element of group iv of the periodic system of elements A wound dressing comprising one or more absorbent elements capable of absorbing wound exudates, a non-steroid anti-inflammatory pain-killing agent and a complex of silver ion and a transitional element of group IV of the periodic system of elements.
EP2429526A1 Ranolazine for the treatment of cns disorders The present invention relates to a method for CNS disorders such as epilepsy and migraine comprising the administration of a therapeutically effective amount of ranolazine.
WO2011163483A3 Polymers for biomaterials and therapeutics Described herein are inventive compositions and methods relating to polymer conjugates and, in particular, to polymer conjugates having pendant side groups comprising ring moieties. In one aspect, embodiments are generally related to compositions that mimic naturally- occurring polyphenol compounds. The compositions comprise, in some embodiments, a polymer backbone having a plurality of hydroxyaromatic pendant side groups or derivatives thereof. For example, in some cases, a pendant side group may be a phenol or a substituted derivative thereof. In some cases, the pendant side group may be an oxidized hydroxyaromatic group, such as a quinone. In some embodiments, self-assembled structures comprising one or more of the polymer conjugates are provided. For example, the polymer conjugates may be combined with a complexing agent to form a particle. In some cases, a polymer conjugate may form a hydrogel. In some embodiments, the self-assembled structures may contain an agent, such as a pharmaceutically active agent. Also provided are methods and kits for forming the compositions, methods of using the compositions, and the like.
US20110092549 Treatment of Sepsis with 5-Ethyl-1-Phenyl-2(1H)-Pyridone A pharmaceutical composition comprising 5-ethyl-1-phenyl-2-(1H)-pyridone (5-EPP) and its use for the treatment of sepsis are disclosed.
US7232814 Heterocyclic carboxy amines such as 9-nitro-7,12-dihydroindolo (3,2-d)(1)-benzazepin-6(5H)-one, used as inhibitors of glycogen synthase kinase-3 beta or cyclin dependent kinases The invention concerns the use for producing of GSK-3β inhibiting medicines from paullone derivatives. The invention is useful for treating pathologies involving GSK-3β and CDK5.
WO2012025811A1 Indolylpyrimidines as modulators of gpr119 The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions modulated by GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).
CN102048759A Gamuzhuer vagina tablet and preparation method thereof The invention discloses a Gamuzhuer vagina tablet and a preparation method thereof. The Gamuzhuer vagina tablet comprises the following components in percentage by weight: 5-75% of Gamuzhuer, 0-30% of biological adhesive, 0-90% of bulking agent, 0.1-10% of disintegrating agent and 0.1-10% of lubricating agent. The invention combines the biological adhesive and the Gamuzhuer, so that the tablet can be disintegrated and attached to the focal part in a shorter time, thereby achieving the purpose of treatment.
CN102018723A Preparation method for marine microorganism natural and polymorphic arsenic compound extract for inhibiting tumors and application thereof The invention discloses a preparation method for marine microorganism natural and polymorphic arsenic compound extract for inhibiting tumors, comprising the following steps of: (1) preparing fine arsenic mineral powder for extracting; (2) metabolizing the ultrafine arsenic mineral powder by marine microorganisms to obtain arsenic extract. The invention also discloses the application of the arsenic compound extract in antitumor drugs. The active components of the antitumor drugs of the arsenic compound extract are specific. Compared with similar and first-line anticancer compound arsenious acids, the arsenic compound extract has the characteristics of enhanced effect and reduced toxicity.
CN102532039A Application of 5-fluoropyrimidine-4(3H)-ketone compound in preparation of anti-tumor medicaments The invention provides an application of a 5-fluoropyrimidine-4(3H)-ketone compound as shown in a formula (I-1) in the preparation of anti-tumor medicaments, especially in the preparation of anti-endometrial carcinoma medicaments. The invention provides a new anti-tumor medicament with obvious anti-tumor activity so as to provide a research basis for screening of the new medicaments and achieve great application prospects; and furthermore, the preparation process of the compound is simple and conductive to industrial production.
WO2011077587A1 Composition for inhibiting allergic diseases Disclosed is a composition for inhibiting allergic diseases, which is capable of inhibiting or ameliorating various symptoms of allergic diseases. Specifically disclosed is a composition for inhibiting allergic diseases, which contains an isothiocyanate and a fragrance material as active ingredients. The composition for inhibiting allergic diseases is characterized in that the isothiocyanate is composed of one or more substances selected from the group consisting of ω-methylthioalkyl isothiocyanate, ω-methylsulfinylalkyl isothiocyanate, ω-methylsulfonylalkyl isothiocyanate and ω-alkenyl isothiocyanate, and the fragrance material is composed of one or more substances selected from the group consisting of indoles, ethers, esters, ketones, fatty acids, aliphatic higher alcohols, aliphatic higher aldehydes, aliphatic higher hydrocarbons, thioethers, thiols, terpene hydrocarbons, phenol ethers, phenols, furfurals, aromatic aldehydes, aromatic alcohols, lactones, furans and natural fragrance materials.
US7410996 3-aryloxy/thio-2,3-substituted propanamines and their use in inhibiting serotonin and norepinephrine reuptake There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof with the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR3 and X is optionally substituted phenyl then A is —S—.
DE102010026090A1 Preparing a matrix for a sublingual dosage form, preferably a tablet, comprises preparing a mixture of gum arabic and active ingredients, and extruding the obtained mixture Preparing a matrix for a sublingual dosage form, preferably a tablet, comprises preparing a mixture of gum arabic and one or more active ingredients, and extruding the obtained mixture. An independent claim is included for the matrix for a sublingual dosage form, preferably a tablet, obtained by the above process.
US20100008998 Submicron nanoparticle of poorly water soluble camptothecin derivatives and process for preparation thereof The present invention relates to a nanoparticle composition comprising a camptothecin derivative, solid polyethyleneglycol and an anti-associative agent, and the process for preparing the same. Specifically, the present invention provides a composition comprising a nanoparticle of the camptothecin derivative, which is prepared by solid-dispersing the poorly water soluble camptothecin derivative in polyethyleneglycol and dissolving the solid dispersions in an aqueous solution containing an anti-associative agent. The composition of the present invention stabilizes the camptothecin derivative lactone form in body fluid for effective anticancer activity.
CN102659889A Preparation of 23, 24-dihydro-epi-iso-cucurbitacin D and use in antitumor drug thereof The tile of the invention is preparation of 23, 24-dihydro-epi-iso-cucurbitacin D and use in antitumor drug thereof. The invention belongs to a natural pharmaceutical chemistry field. The invention mainly discloses a preparation method of 23, 24-dihydro-epi-iso-cucurbitacin D and a use in medicaments for treating tumor diseases thereof. The preparation method is recrystallizing an extract of citrullus colocynthis schrad in chloroform through a combination of silica gel column chromatography and Sephadex LH-20 column chromatography to prepare 23, 24-dihydro-epi-iso-cucurbitacin D. The 23, 24-dihydro-epi-iso-cucurbitacin D can be used as a single preparation or a combination with medicinal dressing to prepare antitumor drugs for treating ovarian cancer, prostatic cancer, oral epidermoid cancer, and gastric cancer.
CN201542233U Multifunctional shape-protecting health care medical pillow for babies The utility model provides a multifunctional shape-protecting health care medical pillow for babies, which includes a pillow inner cover (4) and a pillow inner in a flat dumbbell shape, and the utility model is characterized in that, the pillow inner cover is made from bamboo fiber or fiber modified sanitary finished antimicrobial deodorant fiber fabric, and the pillow inner is composed of multiple connected up medicine cavity bags (2), multiple connected down medicine cavity bags (1), an isolation cloth (5) and a filler (3), and a double-layer isolation cloth (5) is used for isolating multiple connected up medicine cavity bags (2) and multiple connected down medicine cavity bags (1), and a filler (3) is equipped between the double-layer isolation cloth (5). The utility model can prompt normal skull development, and has the functions for protecting skull, correcting flat head, inclined head, square head, tip after-brain and other developmental deformities, developing intelligence, promoting development, preventing disease, improving health-care or the like, and the pillow is safe, effective without toxic and side effects.
WO2012160464A1 Heterocyclic compounds as protein kinase inhibitors The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A' B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.
US20060034781 Peroral preparation for prevention or treatment of atopic dermatatis In accordance with the present invention, a peroral preparation, food and drink, feed, food additive or feed additive for prevention or treatment of atopic dermatitis comprising hydroxyproline or N-acylated derivative of hydroxyproline or a salt thereof is able to be provided and, particularly, said peroral preparation, food and drink, feed, food additive or feed additive comprising 0.1 to 90% by weight of hydroxyproline or N-acylated derivative of hydroxyproline or a salt thereof is able to be provided.
WO2010103204A1 Metal ion chelating agents, methods for preparing same and uses thereof The invention relates to compounds that can be used as metal ion chelating agents or as pollution control agents, having general formula (I), to precursor compounds having formula (II) and to labeled compounds having formula (III). The present invention also relates to the use of compounds (I), (II) or (III) as drugs and to the use thereof for diagnosing, preventing and treating neurodegenerative diseases such as Wilson's disease and Alzheimer's disease.
US20110286917 Novel, Prostate-Specific Gene for Diagnosis, Prognosis and Management of Prostate Cancer Disclosed are nucleic acid and amino acid sequences encoded by a novel, prostate specific gene (UC41) and diagnostic techniques for the detection of human prostate cancer utilizing such nucleic acid and amino acid sequences. Genetic probes and methods useful in monitoring the progression and diagnosis of prostate cancer are described. Methods of treatment for prostate cancer utilizing antisense constructs or antibodies specific for UC41 gene products are also described.
US20120142707 Modified c-3 betulinic acid derivatives as hiv maturation inhibitors Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 betulinic acid and other structurally related natural products derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
WO2009155042A1 3-substituted-1h-indole compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses The invention relates to 3-substituted-1 H-indole compounds of the Formula (I): or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds for the treatment of PI3 and mTOR kinase-mediated diseases, e.g. cancer.
WO2012102583A1 Pharmaceutical composition comprising pyridone derivatives A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
CN101837012A Method for preparing iron wine The invention discloses a method for preparing iron wine, which comprises the following steps of: taking an iron wine block, putting the iron wine block into a large cup of white spirit, and removing iron to obtain the iron wine. The iron wine can treat the deafness by using a magnet to dredge the blocked ears during drinking.
WO2009111277A9 Imidazo [4. 5-b] pyridine derivatives used as raf inhibitors Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
US7947677 Spirolactam tricyclic CGRP receptor antagonists Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, J, K, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
US20090155281 Methods of using antibodies that bind both bcma and taci Molecules that interfere with the binding of a tumor necrosis factor receptor with its ligand, such as a soluble receptor or an anti-receptor antibody, have proven usefulness in both basic research and as therapeutics. The present invention provides antibodies that bind two tumor necrosis factor receptor family members: the transmembrane activator and calcium modulator and cyclophilin ligand-interactor (TACI) receptor, and the B-cell maturation (BCMA) receptor.
CN103027901A Capsaicin chitosan microsphere-carried enteric coated tablet and preparation method thereof The invention discloses a capsaicin chitosan microsphere (CCMS)-carried enteric coated tablet, comprising a CCMS tablet core and a coating film, wherein the CCMS tablet core comprises CCMS, a binding agent, a lubricating agent and a disintegrating agent; and the coating film comprises EudragitL100, a plasticizer, talcum powder and 95% alcohol. The capsaicin (CAP) is a natural product extracted from hot peppers, and the capsaicin can promote lipid metabolism in human body, reduces fat accumulation in body and realizes better weight reducing and blood fat reducing effects. However, the CAP is strongly irritant to the stomach, after the CAP is prepared into chitosan microspheres, the dosage of the CAP can be reduced, and consequentially, the irritation effect on the stomach is reduced; moreover, a film coating technology is used, the medicine releases after being located in small intestine, thus, the compliance to the patient is increased. In addition, the invention provides a preparation method of the CCMS enteric coated tablet, the preparation method is mainly improved in the coating preparation process, so that the preparation technology is simple and reasonable.
US20090054516 Composition for treating cancer cells and synthetic method for the same A pharmaceutical composition having a cytotoxic effect to a cancer cell and a method for the same are provided. The pharmaceutical composition comprises a flavonoid compound having at least one of the following formulas: wherein B ring is a 4-oxo-cyclohexa-2,5-dienyl group, and any one of R1-R12 is one selected from a group consisting of hydrogen group, hydroxyl group, C1-C20 alkyl group, C1-C20 ether group, C1-C20 ester group, carboxyl group, halogen and sugar.
CN1724527A Application of fraxiketone as medicine for treating liver disease The invention relates to the use of Fraxinellone as medicament for treating hepatic diseases, wherein the Fraxinellone is separated from the velamen of Dictamnus dasycorpus Turcz, the Fraxinellone can substantially improve acute hepatic injury in mouse induced with CCl4, D-galactosamine and lipopolysaccharide, in addition, the Fraxinellone can substantially inhibit the release of glutamate-pyruvate transaminase in CCl4 induced mouse primary culture hepatocytes injuries, thus can be used as a novel medicament for treating hepatic diseases.
CN102133212B Asarone medical composition The invention discloses an asarone medical composition. The composition comprises asarone, phospholipid, bile salt and amino acid and is a micellar solution. Furthermore, the invention discloses a preparation method of the medical composition solution and application of a preparation prepared from the medical composition. The experiments conducted by the applicant prove that the problem that the asarone has less possibility of being dissolved in water is solved by adopting the medical composition, and the obtained medical composition has good stability and is suitable for industrial production.
WO2011041300A1 Reduced-odor polyol composition and method of producing same A reduced-odor polyol composition for gastrointestinal lavage of a mammal comprises a polyol and at least one acid salt formed from a reaction between a basic catalyst and citric acid. The reduced-odor polyol composition is produced by providing at least one alkylene oxide; providing at least one initiator; reacting the at least one alkylene oxide with the at least one initiator in the presence of a basic catalyst to produce a polyol; and neutralizing the basic catalyst with citric acid, thereby forming at least one acid salt and producing the reduced-odor polyol composition.
WO2011036533A1 Pharmaceutical composition comprising prasugrel and triflusal The present invention relates to pharmaceutical composition for oral administration comprising prasugrel or its salt and triflusal, as well as to a process for preparation of such composition, and use of such composition for treating a platelet aggregation disorder in a subject.
EP1896015A1 Methods and compositions for the treatment of autoimmune and inflammatory diseases associated with toll-like receptors The present invention relates to the treatment of autoimmune and/or inflammatory diseases associated with overexpression of Toll-like receptor 3 (TLR3) as well as Toll-like receptor 4 (TLR4) and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. This invention also relates to the use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune and inflammatory diseases associated with Toll-like receptor 3 (TLR3) as well as Toll-like receptor 4 (TLR4) and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. This invention also relates to treating a subject having a disease or condition associated with abnormal Toll-like receptor 3 as well as Toll- like receptor 4 and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. The present invention also relates to the treatment of autoimmune-inflammatory pathologies and chemokine and cytokine-mediated diseases associated with TLR overexpression and signaling. This invention also relates to pharmaceutical formulations capable of inhibiting the IRF-3/Type 1 IFN/STAT/ISRE/IRF-1 pathway associated with Toll-like receptor overexpression or signaling.
US7662948 Antisense oligonucleotides against VR1 Antisense oligodeoxynucleotides against VR1, corresponding nucleotide constructs, cells containing said nucleotide constructs, pharmaceutical and diagnostic substances, uses thereof in pain therapy, and methods for diagnosing symptoms related to VR1 and for identifying pain-modulating substances.
EP2559691A1 Thiophene analogues for the treatment or prevention of Flavivirus infections The present invention relates to compounds represented by formula IA or pharmaceutically acceptable salts and solvates thereof which are useful for treating flaviviridae viral infections wherein R1 is C1-6alkyl or C3-6 cycloalkyl; X is M is R5 is cyclohexyl which is unsubstituted or substituted one or more times by R13; R6 is or cyclohexyl which is substituted in the 4 position by R14; and Y, R14a and R14 are as defined herein.
WO2012008467A1 Pharmaceutical composition for promoting osteogenesis containing axial-equatorial aryl-oriented furofuran-type lignan, and pharmaceutical preparation, functional food product, and health food product comprising composition Provided is a composition that, even when used in a very small amount, has the effect of improving bone density and promoting bone growth, and has few side effects, and also provided are a pharmaceutical preparation for promoting bone growth, functional food product, and health food product containing the composition as an active ingredient. The composition can be obtained from any plant part selected from the group consisting of the bud, leaf, bark or wood of a plant belonging to the family Magnoliaceae. The composition comprises at least one selected from the group consisting of fargesin and physiologically acceptable salts, hydrates, and glycosides thereof. The pharmaceutical preparation, functional food product, and health food product comprising this composition as an active ingredient sufficiently improve bone density and promote bone growth, even when used in small amounts, and therefore realize preventive and/or therapeutic effects against bone disease etc. such as osteoporosis.
CN103230382A Celecoxib effervescent tablet and preparation method thereof The invention discloses celecoxib effervescent tablets which are used for treating rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. The tablets can also be used for treating acute pain, dysmenorrhea, colorectal polyps and post-operative analgesia, lower back pain, shoulder periarthritis and tenosynovitis. According to the invention, celecoxib is adopted as a raw material, and auxiliary materials are added, such that the celecoxib effervescent tablets are prepared. The celecoxib effervescent tablets have the advantages of fast disintegration, fast absorption high bioavailability, convenient application, low intestinal residue, low side effect, and sweet taste and good fragrance. With the tablets and the method, patient medication compliance can easily be improved.
CN101597231B NO donor medicine and synthesis method thereof The invention discloses a NO donor medicine expressed by general formula (I) and synthesis method thereof. The invention utilizes danshensu with functions of lipid peroxidation resistance and free radical clearing to be bonded with a NO donor structure, so as to form a novel medicine; the medicine molecules are capable of releasing NO while clearing oxygen free radical, have obvious prevention and treatment effect on ischemia/reperfusion injury, and can effectively reduce myocardial infarction range, so as to greatly reduce CK and LDH activities and MDA concentration in serum.
CN102153548B Analogue nucleoside derivative containing thiazolidone (thiazinidone) ring, preparation method and application thereof to medicinal preparations The invention discloses an analogue nucleoside derivative containing a thiazolidone (thiazinidone) ring, a preparation method and application thereof to medicinal preparations. The preparation method comprises the following steps of: a, dissolving fatty amine or aromatic amine (1) and furfural (2) which serve as initial raw materials in absolute methanol solvent with stirring according to a molarratio of 1.2:1; and b, performing microwave radiation or stirring at the room temperature, adding mercaptoacetic acid or mercaptopropionic acid according to a molar ratio of 1:2 and reacting, and regulating the pH value to be between 6.5 and 7.5 to obtain a compound shown as a chemical general formula (I).
CN103316100A Chinese-western compound preparation for treating chicken colibaciuosis The invention relates to a Chinese-western compound preparation for treating chicken colibaciuosis. A powder is prepared through drying, crushing and mixing levofloxacin, an Isatis Root extract, Rhizoma Coptidis, Radix Scutellariae, Anemone chinensis and purslane according to a certain ratio. The use method of the preparation is characterized in that 3g of the preparation is used by each chicken for 1-2d; or 1-2% of the preparation is uniformly mixed in a feed, and the obtained feed mixture is taken by the chicken for 1-2d; or 3g of the preparation is added with warm water and is immersed for 1h, and the obtained water mixture is drunk by the chicken for 1-2d. The total effective rate of the preparation on the chicken colibaciuosis reaches above 80%.
US20100035807 Composition and method for treatment of tumors The present invention relates to a composition which is useful in the treatment of a tumor, a method for making such a composition, and a method for using such a composition. The invention relates also to a method for assaying for inhibitors of the activity of Core 1 protein and/or other proteins of the respiratory complex III of mitochondria.
US7199114 Triterpene quaternary salts as biologically active surfactants The invention provides novel compounds that are quaternary amine derivatives of betulin and other triterpenes. The compounds have antibacterial, antifungal, and surfactant properties.
US20100144645 Compositions and methods for enhancing analgesic potency of covalently bound-compounds, attenuating its adverse side effects, and preventing their abuse The invention generally relates to compositions and methods with covalently bound compounds, such as controlled substances covalently attached to a chemical moiety, and opioid antagonists or covalently bound opioid antagonists to enhance analgesic potency and/or attenuate one or more adverse effects of covalently bound compounds, including adverse side effect(s) in humans such as nausea, vomiting, dizziness, headache, sedation (somnolence), physical dependence or pruritis. This invention relates to compositions and methods for selectively enhancing the analgesic potency of a covalently bound compound and simultaneously attenuating anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects associated with the administration of a covalently bound compound. The methods of the invention comprise administering to a subject an analgesic or sub-analgesic amount of a covalently bound compound and an amount of excitatory opioid receptor antagonist such as naltrexone or nalmefene effective to enhance the analgesic potency of a covalently bound compound and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of covalently bound compound. The invention also relates to the addition of covalently-bound opioid antagonists to the compositions containing covalently bound compounds such that if the compositions are subjected to manipulation by illicit chemists, the opioid antagonist is released effectively reducing or eliminating the euphoric effect of the covalently bound compounds.
WO2009114981A1 Process for preparing sulfoxide compounds Disclosed are a process for preparing a chiral sulfoxide compound of general formula I as a single enantiomer or in an enantiomerically enriched form, and S-(-)-levo-omeprazole, S-(-)-levo-pantoprazole and S-(-)-le vo-lansoprazole prepared thereby. Formula (I) omeprazole: R 1=CH 3, R 2=OCH 3, R 3=CH 3, R 4= R 6= R 7=H, R 5=OCH 3 lansoprazole: R 1=H, R 2=OCH 2CF 3, R 3=CH 3, R 4= R 5= R 6= R 7=H pantoprazole: R 1=H, R2=OCH 3, R 3=OCH 3, R 4= R 6= R 7=H, R 5=OCHF 2
US7378411 Substituted thienopyrimidinones as a mitotic kinesin inhibitor The present invention relates to thienopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
CN101099741A Alprostadil and vitamin F millimicroball composite medicine and its preparation method The present invention relates to a millimicrosphere composite medicine containing mixture of alprostadil and vitamin F and its preparation method. The invented medicine can greatly prolong the half-life time in vivo and has good target action for tumor.
US20090018151 Topical Treatment of Peripheral diabetic complications This invention relates to agents for treating, ameliorating, or preventing diabetic complications specifically diabetic neuropathy and skin ulceration by topical application of materials containing one or more arterial or venous dilation components and one or more fast sodium channel inhibitors. Particularly, the invention relates to treating or ameliorating agents that contain minoxidil and its related congeners, which have both potassium channel agonist properties and nitric oxide agonist properties as an active ingredient and which are effective against diabetic complications such as neuropathy, peripheral circulation disorders and skin ulcerations. Unique methods of delivery including delivery through impregnated socks or gloves to match the distribution of pain are also noted.
CN103304579A ortho-positioned bridged azacrown ether modified phthalocyanin and preparation method and application thereof The invention discloses a ortho-positioned bridged azacrown ether modified phthalocyanin, and a preparation method and application thereof, and belongs to the field of optically functional material preparation. The compound provided by the invention has unique ortho-positioned bridged azacrown ether modification characteristic, and is clear in structure and unique in synthesis route. The compound provided by the invention is a multifunctional molecule which can be taken as both a photosensitive drug and a metal ion spectrum probe. As the photosensitive drug, the photosensitization ability of the compound is high; and as the spectrum probe, the compound can be used for selective identification to Fe<3+> and Cu<2+> ions.
CN101036714B Medicinal composition for treating and/or preventing diabetes The invention relates to a drug or a functional health product composition, a preparing method and use thereof. The composition has a natural plant extract or a monomer as an active ingredient. The drug composition of the invention is applicable for treating and preventing diabetes.
WO2009023355A3 Compositions and methods for reducing the toxicity of certain toxins Compositions and methods for reducing the toxic effect of certain peptide toxins by administering an agent that directly or indirectly reduces disulfide bonds that are important for maintaining the toxin in an active conformation. Also described are compositions and methods for reducing the toxic effect of toxins that contain a heavy metal using an agent that destabilizes the binding of a metal ion that is important for toxin activity.
US20080167322 Substituted Pyrazoles as Modulators of Chemokine Receptors Substituted pyrazole compounds such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
CN101073664A Uso of W-peptide in treatment of tumor The invention is concerned with the purpose of the W peptide in anti-knubbly medicine preparation. W peptide, as a kind of hexad peptide, its amino acid order is: Trp-Lys-Tyr-Met-Val-D-Met, with the ability of inhibits the growing and forming of the knubbly, as the W peptide, as the igand of the specificity of the formyl peptide receptor 1 integrates with the FPRL 1 that makes the receptor acticating and aroses the endogenesis TRAIL tends to increase, thereby the specificity destroys the knubbly cell. The inventor has also discovered that the W peptide can use with the exogenous TRAIL together and brings the destroy effect to the knubbly cell up to one more stage.
CN103601684A 5-arylselenobenzimidazole compound and application thereof The invention belongs to the technical field of medicine and relates to a 5-arylselenobenzimidazole compound and application thereof, specifically to the compound and application of the compound as a tumor cell proliferation inhibitor in preparation of antineoplastic drugs. The objective of the invention is to design and synthesize an analogue of Combretastatin A-4 with good antineoplastic activity, i.e., the 5-arylselenobenzimidazole compound. The synthesized compound presents good results in in-vitro and in-vivo antineoplastic activity tests.
EP1077678A4 Mucoadhesive compositions for administration of biologically active agents to animal tissue This invention pertains to mucoadhesive compositions for the delivery of pharmacologically active agents, and to polymeric formulations that allow for a prolonged, sustained release of the active agents. More specially the invention pertains to compositions for the delivery of drugs to mucosal tissue, said composition comprising a drug or a plurality of drugs to be delivered and a thermoplastic graft copolymer, said graft copolymer being the reaction product of a polystyrene macromonomer having an ethylenically unsaturated functional group, and at least one acidic hydrophilic monomer having an ethylenically unsaturated functional group.
CN103638021A Preparation method for pidotimod oral liquid The invention belongs to the technical field of medicine preparation, and specifically relates to a preparation method for a pidotimod oral liquid. The preparation method comprises: adding 50-300 g of sorbitol and 0.1-1 g of an antiseptic into a mixing pot, adding a proper amount of water to dissolve the above components, adding a proper amount of a pH adjusting agent to adjust pH to 4-5, continuing to add 10-60 g of pidotimod and dissolving pidotimod, adding 0.5-5 g of a flavoring agent and 0.1-1 g of a stabilizing agent, adding the pH adjusting agent to adjust pH to 6-7, and finally adding pure water to enable the volume of the solution to be 1000 mL. The preparation method employs water as the solvent, and auxiliary agents are relatively less; and the prepared oral liquid is safe and stable, and has the advantages of being rapidly absorbed after eaten, relatively high in biological availability, high in dispersity, good in mouthfeel, convenient to eat and easy to accept by patients.
US20060094902 Amino acid analogues In the present specification we describe a new class of compounds, designed to modulate the ability of blood vessels to synthesize NO from L-arginine. In particular we have identified novel compounds which enhance the entry of L-arginine into cells. These compounds improve endothelial function, and thereby have the potential to retard the progression of vascular disease in conditions such as hypertension, heart failure and diabetes. This new class of drugs may also have other potentially, relevant pharmacological actions, including anti-hypertensive and anti-anginal actions.
CA2192433C Anti-herpesvirus compounds and methods for identyfying, making and using same This invention relates to methods for inhibiting herpes replication and for treating herpes infection in a mammal by inhibiting the herpes helicase-primase enzyme complex. This invention also relates to thiazolyphenyl derivatives that inhibit the herpes helicase-primase and to pharmaceutical compositions comprising the thiazolylphenyl derivatives, to methods of using and methods of producing the thiazolylphenyl derivatives.
US7812160 G-protein-coupled chemoattractant receptor, expressed on T helper cells antagonists such as [4-(dimethylamino)-2-(4-{[4-(trifluoromethyl)benzoyl]amino}benzyl)-5-pyrimidinyl]acetic acid;, used for the treatment of allergic diseases, inflammatory diseases, eosinophil- and basophil-related diseases The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.
CN101011375A Combretastatin A-4 eye-using preparation for treating diabetic retinopathy The invention relates to a method for using Combretastatin A-4 to prepare the eye agent. The invention uses 95-100% Combretastatin A-4 as material to prepare variable eye agents at 1mg-3g as gutta, paste and gelling agent. The Combretastatin A-4 can restrain the growth of new vessel without side effect and affecting the growth of normal retina vessel. The invention can be used to treat proliferating diabetic retinopathy.
US7341871 Recombinant expression vector comprising promoter sequence, age regulatory sequence; can use in treatment of age-related and liver diseases; operably linking nucleic acid sequence, promoter sequence, and age regulatory sequences to produce a transgene, introducing into cell The invention provides nucleic acid sequences which regulate expression of a nucleotide sequence of interest. In particular, the invention provides nucleic acid sequences which regulate expression of a nucleotide sequence of interest in an age-related manner and/or in a liver-specific manner. The invention further provides methods of using the regulatory nucleic acid sequences provided herein for age-related and/or liver-specific expression of nucleotides seuqences of interest. The invention also provides host cells and transgenic non-human animals which harbor the regulatory nucleic acid sequences of the invention. The compositions and methods of the invention are useful in regulating expression of a nucleotide sequence of interest in an age-related and/or liver-specific manner.
WO2012018773A1 Combinations of beta - 3 adrenergic receptor agonists and muscarinic receptor antagonists for treating overactive bladder Pharmaceutical combinations comprising a beta-3 adrenergic receptor agonist and a muscarinic receptor antagonist, and methods for their use are disclosed. Disclosed combinations include solabegron and oxybutynin. Methods of using the pharmaceutical combinations for the treatment of one or more symptoms associated with overactive bladder, for example, frequency of urgency, nocturia, and urinary incontinence, are also disclosed.
CN1958007A Vagina tablet for treating cervicitis, cervical erosion, and preparation method A vaginal tablet for treating cervicitis and cervical erosion is prepared from phellodendron bark, flavescent sophora root, catechu, baked alum and borneol. Its preparing process is also disclosed.
US20080119471 1-((4-chlorophenoxy)methyl)carbonyl-2-methyl-4-(4-fluorobenzyl)piperazine; chemokine receptor CCR1 antagonist; chemokine (MIP-1 alpha and RANTES) inhibitor; antiinflammatory agent; multiple sclerosis, rheumatoid arthritis Use of a compound of the following formula (Ia): for the production of a medicament for the treatment of endometriosis in human wherein the treatment comprises administering to a human female in need of such treatment a therapeutically effective amount of said compound.
WO2013122920A1 Dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
CN102133186A Racecadotril liposome solid preparation The invention discloses a racecadotril liposome solid preparation. The racecadotril liposome is prepared from racecadotril, soy lecithin, hydrogenated egg lecithin, cholesterol and tween 80 in the weight ratio of 1:2-8: 2-8:1.5-6:0.5-3; and the solid preparation is prepared from the racecadotril liposome and other pharmaceutically common auxiliary materials. The other pharmaceutically common auxiliary materials comprise filler, a disintegrating agent, a sweetener, an adhesive and a lubricant. The racecadotril liposome solid preparation improves the dissolubility of the racecadotril so as to improve bioavailability; a medicament is absorbed and distributed in a body fast; a curative effect is improved obviously; and the product quality of the preparation is improved and the toxic and side effects are reduced.
WO2006121258A1 Composition comprising an obovatol having anti-anxiety activity The present invention relates to obovatol compound isolated from Magnolia obovata Thunb. for the prevention and treatment of anxiety disorders involved with CNS. The obovatol compound isolated from Magnolia obovata Thunb. have potent anti-anxiety activity, verified by an increased percentage of time on the open arms, an increased number of entries into, time spent on, the distal portion of the open arms, and a decreased activity of locomotor. Therefore it can be used as the therapeutics or health care food for treating and preventing anxiety disorders.
WO2014114573A1 Antiviral triazole derivatives The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
US20100216865 MicroRNA COMPOSITIONS IN THE TREATMENT OF VEGF-MEDIATED DISORDERS The invention provides methods of treating diseases caused by the over-production of a VEGF polypeptide by administering miRNA or miRNA inhibitor compositions to decrease at least one activity of a VEGF polypeptide.
CN101538238A Polymorphs of atorvastatin tert.-butylester and use as intermediates for the preparation of atorvastatin The invention relates to crystalline forms 2 of atorvastatin tert.-butyl ester (Formula (II)), processes for their preparation and their conversion to highly pure atorvastatin hemi calcium in non-crystalline, in particular amorphous form.
US20060287339 Aza- and polyazanthranyl amides and their use as medicaments Aza- and polyazanthranyl amides and their use as medicaments in the treatment of diseases caused by persistent angiogenesis are described, as well as the intermediates used in the preparation of the aza- and polyazanthranyl amides.
WO2009024026A1 Gastrodia elata polysaccharide, its sulfated derivative and their preparation and use A gastrodia elata polysaccharide extracted from gastrodia elata Blume, its extraction method are disclosed. The invention also discloses the sulfated derivative of said polysaccharide and its preparation. The data of in vitro test shows that the sulfated derivative of said polysaccharide can inhibit dengue fever virus evidently, especially inhibit dengue fever virus type II. Therefore, it can be used as inhibitor of dengue fever virus type II and can be used as a medicine in therapy of anti-infection of dengue fever virus.
CN1895547A Medicine for treating diabetes and its preparation A medicine for treating diabetes B and its complications is prepared from gliquidone and 21 Chinese-medicinal materials including ginseng, astragalus root, rehmannia root, red sage root, etc. Its preparing process is also disclosed.
WO2014102589A1 Quinazolin-4(3h)-one-type piperidine compounds and uses thereof The present disclosure relates to Quinazolin-4(3H)-one-Type Piperidine Compounds, such as those of Formule (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, Q, Y1, Z, A, B, E, and a are as defined herein; compositions comprising an effective amount of a Quinazolin-4(3H)-one-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Quinazolin-4(3 H)-one-Type Piperidine Compound.
CN102499925A Neutrophilic granulocyte elastase inhibitor The invention discloses a neutrophilic granulocyte elastase inhibitor of which the active ingredient is a compound with a pentacyclic triterpene structure. The inhibitor can be used for preparing a medicament or health-care food for treating or preventing diseases with neutrophilic granulocyte elastase as an action way. The diseases with the neutrophilic granulocyte elastase as an action way include acute lung injury, acute respiratory distress syndrome, systemic inflammatory response syndrome and cystic fibrosis diseases. As the active ingredient of the neutrophilic granulocyte elastase inhibitor disclosed by the invention, the compound with the pentacyclic triterpene structure can be extracted and separated from a natural product or can be prepared from a natural product through chemical synthesis, and has the advantages of being wide in sources, safe and effective.
WO2006091187A1 Isoflavonoids for preventing radiation- and chemotherapy- induced weight loss Methods to ameliorate weight loss and facilitate weight gain during recovery from chemotherapy, radiation therapy (or both chemotherapy and radiation therapy) treatment regimens are provided.
CN101732335A Ointment medicament for treating acne and production method thereof The invention relates to an ointment medicament for treating acne. The ointment medicament is prepared by mixing 128 to 160 grams of metronidazole, 12 to 15 grams of erythromycin, 4 to 5 grams of vitamin B6 and an oil phase substrate and a water phase substrate, wherein the oil phase substrate consists of 120 to 200 grams of stearic acid, 50 to 100 grams of glyceryl monostearate, 0 to 200 grams of liquid paraffin and 0 to 200 grams of castor oil; the water phase substrate consists of 320 to 450 grams of distilled water, 100 to 200 grams of glycerin, 2 to 15 milliliters of triethanolamine, 1.5 to 2 grams of lauryl sodium sulfate and 0 to 50 grams of stearyl alcohol; the metronidazole has the effect of resisting broad-spectrum anaerobion; metabolites generated when the metronidazole is reduced in a human body also have the effect of resisting anaerobion; antimicrobial spectrum of the erythromycin is similar to that of penicillin; and the vitamin B6 in an erythrocyte is pyridoxal phosphate which is used as a coenzyme indispensable to an organism, can participate in normal metabolism of amino acid, carbohydrate and fat, can also participate in the reaction of converting nicotinic acid into 5-hydroxytryptamine by tryptophan, can stimulate the growth of leukocytes, and is a substance needed for forming ferrohemoglobin.
WO2013088335A1 Crystalline form of cabazitaxel and process for preparing the same The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3- phenylpropionate and process for preparing the same.
WO2012071611A1 Histone inhibition The invention relates to a method of inhibiting the cytotoxic activity of extracellular histones in a subject, comprising administering an effective amount of a polyanion to the subject. In particular the invention relates to a method for the treatment of patients who are suffering from sepsis and employs polyanions to rapidly form complexes with and thus neutralize or inhibit the cytotoxic activity of extracellular histone proteins, for example, those found in the blood circulation of sepsis patients.
EP2550973B1 Wound spray The present invention refers to a composition, comprising hemoglobin or myoglobin, wherein in at least 40% of said hemoglobin or myoglobin the oxygen binding site is charged by a non-O 2 ligand, and at least one further ingredient, a method for preparing said composition and the use of hemoglobin or myoglobin charged with a non-oxygen ligand for external treatment of wounds.
US20100239562 Kv CHANNELS IN NEURODEGENERATION AND NEUROPROTECTION A family of potassium channels (Kv) are expressed in neurons when they are damaged. Blockers of these channels protect neurons from several different types of insults, whether due to disease or trauma. Furthermore, blockers of these channels promote neurite outgrowth in neural progenitor cells. These findings permit methods of treating as well as methods for identifying and developing drugs for neurological diseases where injury to neurons may occur.
WO2013026587A1 1,4 disubstituted pyrrolidine - 3 - yl -amine derivatives and their use for the treatment of metabolic disorders Therapeutic compounds are disclosed having the general formula (I) that are useful for the treatment of metabolic disorders, including type II diabetes. The compounds have activity as agonists of GPR1 19. Compounds having stereochemistry of formula (la) may also demonstrate DPP-IV inhibitory activity.
CN102499937A Application of the combination of deoxynucleosides and nucleosides in preparation of antitumor drugs The invention discloses application of the combination of deoxynucleosides and nucleosides in preparation of antitumor drugs, wherein the deoxynucleosides comprise deoxyadenosine, deoxyguanosine, deoxycytidine and thymidine; and the nucleosides comprise adenosine, guanosine, cytidine, uridine, deoxyadenosine, deoxyguanosine, deoxycytidine and thymidine. The advantages of the invention are that the drugs prepared from the combination of deoxynucleosides and other nucleosides, for treating a variety of malignant tumors such as gastric cancer, lung cancer, liver cancer, colon cancer, breast cancer, genital system cancer, have obvious antitumor effects, high efficacies, broad spectra and low toxicities. Compared with utilization of a single drug, utilization of drugs in combined way lowers the concentration of single drugs in blood so as to reduce the toxic side effects; and the occurrence of drug resistance in tumors may be delayed.
EP2509592A1 Bibw 2992 for use in the treatment of triple negative breast cancer The present invention relates to a method of treating patients suffering from triple negative breast cancer comprising administration of an effective amount of the irreversible EGFR/HER1 and HER2 inhibitor BIBW 2992 (1) to a person in need of such treatment, optionally in combination with the administration of a further chemotherapeutic agent (2), in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery.
CN101085284A Tinea unguium grease The invention discloses a tinea unguium grease which is prepared from the following medicinal herbs (by weight ratio): chaulmoogra seed 100g, licorice root 60g, roor of sessile stemona 30g, flavescent sophora root 30g, cnidium fruit 30g, apricot kernel 40g, pricklyash peel 15g, ledebouriella root 15g, safflower 15g, sulfur flour 20g and dahurian angelica root 20g.
WO2010113952A1 Muscarinic receptor antagonist Disclosed is a compound represented by formula (1). The compound is a novel imidazolium derivative having an excellent antagonistic activity on a muscarinic M3 receptor and having excellent effectiveness, long-lasting efficacy and safety. The compound is a prophylactic or therapeutic agent for various diseases associated with airflow obstruction, such as chronic bronchial asthma, chronic obstructive pulmonary disease (COPD), asthma, chronic airway obstruction, fibroid lung, pulmonary emphysema, diffuse panbronchiolitis, bronchiectasis, idiopathic interstitial pneumonia and rhinitis.
CN102702382A Preparation method of chitosan derivative and application in anticoagulant drug The invention relates to a preparation method of a chitosan derivative, which particularly comprises the following preparation steps: dropwisely adding chlorosulfonic acid into dimethyl formamide with a volume ratio of the chlorosulfonic acid and the dimethyl formamide being 1-6:10-40, uniformly stirring, heating to 30-50 DEG C, adding monocholesterylsuccinate chitosan, stirring and reacting for 12-18 hours, dropwisely adding a sodium hydroxide solution with a mass fraction of 10-30%, neutralizing the solution to obtain a pH value of 6-8, filtering to obtain a filtrate to keep in reserve; dialyzing the obtained filtrate, performing freeze drying after dialysis to obtain the chitosan derivative. The invention also relates to an application of the chitosan derivative in anticoagulant drugs. The synthetic process of the invention is easy to operate, simple and easy to obtain the product, suitable for industrial large-scale production, high in industrialization degree, less in investment and development cost, and provides a good ocean new drug with potential value.
WO2008102374A1 Amorphous form of docetaxel A process for preparation of Amorphous Form of Docetaxel comprising: i. preparation of a solution or suspension of Docetaxel in an organic solvent or mixtures thereof; ii. evaporation of the solvent or mixtures thereof from the solution or suspension of step i ) under reduced pressure to obtain a solid substance; iii. optionally further dissolving or suspending the solid substance of step ii) in an organic solvent or mixtures thereof and evaporation of the solvent or mixtures thereof from the solution or suspension under reduced pressure to obtain a solid substance; iv. further optionally repeating step iii) one or more times; v. drying the solid substance obtained from step ii), iii) or iv) to give the amorphous form of Docetaxel. An amorphous form of docetaxel obtained by the process. A composition comprising amorphous form of Docetaxel along with pharmaceutically acceptable excipients adapted for therapy for cancer of various origins.
WO2006085689A1 Anticancer agent to be combined with telomelysin It is intended to provide a medicinal composition having an enhanced anticancer activity. More specifically speaking, a medicinal composition to be used in a combination therapy for tumor which comprises a polynucleotide of a recombinant virus containing a human telomerase promoter, E1A gene, IRES sequence and E1B gene in this order and a substance having an antitumor effect.
US20070270422 Aromatic Compounds The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X1 represents a nitrogen atom or a group —CH═; R1 represents a group -Z-R6, wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R4 represents an imidazolyl lower alkyl group or the like.
US7309691 Combined pharmaceutical preparation containing LHRH-analogous substances and anti estrogens for treating gynaecological disorders The invention relates to a pharmaceutical combined preparation of LHRH analogues and anti-oestrogens having tissue-selective oestrogen activity and also to its use for the treatment of gynaecological disorders, especially for the treatment of endometrioses and myomas.
CN102727447A Florfenicol controlled release preparation and preparation method thereof The invention discloses a florfenicol controlled release preparation and a preparation method thereof and belongs to the field of veterinary drug technology. The florfenicol controlled release preparation mainly comprises, by weight, florfenicol, sustained and controlled release materials and other auxiliary materials and can be made in forms of tablets, pills, granules, framework controlled release preparation of capsules, membrane controlled release preparation or osmotic pump controlled release preparation. The florfenicol controlled release preparation has a reasonable scientific formula, safe and high efficient auxiliary materials, strong adaptability, advanced technology, safe quality, good stability, reduces peak-valley phenomena of blood drug concentration, maintains stably the effective blood drug concentration for 24 hours, reduces toxic side effects of medicines, and widens a usage scope of the florfenicol.
US8389279 α-aminocyclolactam ligands for G-protein coupled receptors, and methods of using same The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (I) wherein y is any integer from 1 to 8; z is any integer from 0 to 8 with the proviso that y and z cannot simultaneously be 1; X is —CO—(Y)k—(R1)n or SO2—(Y)k—(R1)n; k is 0 or 1 Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or Y is a cycloalkenyl or polycycloalkenyl group; each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, alkylamino, alkylaminoalkyl, alkylaminodialkyl, charged alkylaminotrialkyl or charged alkylcarboxylate radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl, charged aminotrialkyl, or carboxylate radical; and n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y; or alternatively R1 may be selected from a peptido radical, for example having from 1 to 4 peptidic moieties linked together by peptide bonds (for example a peptido radical of 1 to 4 amino acid residues).
US7718648 Pyridobenzazepine compounds and methods for inhibiting mitotic progression This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
CN101768612A Preparation method of nitrobenzene derivatives and application thereof The invention relates to a preparation method of nitrobenzene derivatives extracted and separated from culture solution of marine endophytic fungus and application in preparation of anticancer drug thereof. Firstly, strain culture of marine endophytic fungus is conducted in the strain medium during preparation, then, fermentation culture is conducted in a fermentative medium, the liquid generated by fermentation is filtered to remove fungus body, and the obtained fermentation solution is extracted with organic solvent; column chromatography or TLC chromatography of the obtained extraction solution are conducted after concentration, the obtained eluant is concentrated to obtain colorless crystals which are nitrobenzene derivatives. The nitrobenzene derivatives provided by the invention has strong inhibitory activity for human nasopharyngeal carcinoma KB and resistant strains KBV200 tumor cells of human nasopharyngeal carcinoma, can be used as anticancer drug; the raw material can be manufactured in large-scale production, and therefore, the application prospect of the invention is wide.
WO2006036015A3 6- (pyridinyl) -4-pyrimidone derivates as tau protein kinase 1 inhibitors A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof:wherein R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom or the like; R3 represents a halogen or the like; q represents an integer of 1 to 7; R4 represents a halogen or the like; p represents 0 or an integer of 1 to 5; R5 represents a C6-C10 aryl, a heterocycle or the like; and X represents oxygen, NH, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
CN101032511A Health wine for conditioning blood sugar and the preparing method The blood sugar reducing health wine includes white liquor and puerarin, astragalus polysaccharide, jasminoidin and/or ursolic acid. Each 500 ml of the health wine contains at least 1 mg of the said health factors. The blood sugar reducing health wine is mellow, stable and controllable in quality, and has the health function of preventing and treating diabetes.
CN1927274A Externally used drug for treating herpes zoster The invention relates to a medicinal composition for herpes zoster which is prepared from the following raw materials (by weight ratio) through conventional processes: seed of cowherb 50-65%, corydalis ambigua 25-40%, and borneol 5-12%.
CA2431515C Composition comprising bisphosphonates for prevention and/or treatment of metabolic diseases of bones, process for preparing such composition, and use thereof The present invention relates to a composition for prevention and/or treatment of metabolic diseases of bones comprising at least one bisphosphonate; viscosity agents comprising carboxymethylcellulose and xanthan gum; at least one flavouring agent; and purified water; a process for preparing a composition according to the present invention; and use of such a composition for prevention, treatment and/or diagnosis of metabolic diseases of bones, especially for children.
US20120245150 NOVEL (HETEROCYCLE/TETRAHYDROPYRIDINE)-(PIPERAZINYL)-1-ALCANONE AND (HETEROCYCLE/DIHYDROPYRROLIDINE)-(PIPERAZINYL)-1-ALCANONE DERIVATIVES, AND USE THEREOF AS p75 INHIBITORS The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof.
CN101434595A Antifungal agent-sulfur chromanone thiosemicarbazone compounds The invention pertains to the technical field of medicaments, more particularly relates to a (sulfur) urea derivative with substituted semicarbazone thiochromanones and provides a novel and efficient antifungal agent. The structural formula of the derivative is shown as the Formula I. The invention also relates to a chemically acceptable compound of the derivative and a medicament combination taking the compound as an active ingredient. As a novel antifungal agent, the compound has relatively strong effect of killing pathomycete commonly seen clinically and is expected to overcome the defects that azoles antifungal medicaments widely used in clinical treatment has serious toxic side effect and is easy to generate medicament resistance, and the like. The compound is prepared by the condensation of substitutable thiochromanones and substitutable semicarbazone (sulfur) in an organic solvent.
US20100069330 Pharmaceutical Compositions and Methods for Preparing and Using Lipophilic Organosulfur Cell Proliferation Inhibitors Novel compositions of lipophilic organosulfur compounds, their preparation and use in methods for treating disease are described. Silicon confers lipophilicity that can enhance the penetration of the silicon derivative compounds across the gut wall, cell membranes and blood brain barrier, thus improving therapeutic properties including bioavailability, metabolism, and/or pharmacokinetics. The organosilyl group provides compounds having improved pharmacokinetics. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, polymorphic forms, crystalline forms or an amorphous form, pharmaceutical compositions and methods for treatment of diseases, maladies or conditions. Also disclosed are processes for making such compounds as well as intermediates useful in such processes.
US6943239 Antigenic fusionprotein carrying Galα1,3Gal epitopes The present invention relates to an antigenic fusionprotein, which carries multiple Galα1,3Gal epitopes. The fusion protein according to the invention may also be comprised of a heavily glycosylated mucin part, which mediates binding to selectins, such as PSGL-1, and a part, which exhibits immunoglobulin properties, such as the Fc part of IgG. The fusionprotein according to the invention is preferably used as an absorber to prevent a hyperacute rejection of a xenotransplant, such as a pig tissue or organ transplanted into a human patient. In addition, the invention relates to a method for the prevention of hyperacute rejection reaction in a patient who is to receive a xenotransplant.
CN103242406A Dehydroepiandrosterone aromatic aldehyde azine steroidal compound and synthetic method thereof as well as application thereof in preparation of anti-tumor drugs The invention relates to a dehydroepiandrosterone aromatic aldehyde azine steroidal compound with an azine structure. The chemical structural formula is as shown by dehydroepiandrosterone acetone azine (1), dehydroepiandrosterone benzaldehyde azine (2), dehydroepiandrosterone-3-pyridylaldehyde azine (3), dehydroepiandrosterone-3-thiophenecarboxaldehyde azine (4), dehydroepiandrosterone-3-hydroxybenzaldehyde azine (5), dehydroepiandrosterone-2-naphthaldehyde azine (6), dehydroepiandrosterone-4-quinolinecarboxaldehyde azine (7) and dehydroepiandrosterone-6-methoxy-naphthaldehyde azine (8) described in the specification. Experiments prove that the dehydroepiandrosterone aromatic aldehyde azine steroidal compound has an obvious inhibitory effect on various tumor cell strains, and can be applied to preparation of drugs for treating cancers.
CN102516247A A-type calcium L-5-methyltetrahydrofolate polymorphism and preparation method thereof The invention provides an A-type calcium L-5-methyltetrahydrofolate polymorphism and a preparation method thereof. The 2 theta angle of an X-ray diffraction pattern of the A-type crystalline at least has diffraction peaks at 6.8 +- 0.2 DEG, 13.5 +- 0.2 DEG, 17.0 +- 0.2 DEG, 19.2 +- 0.2 DEG, 20.4 +- 0.2 DEG, 21.0 +- 0.2 DEG, 28.5 +- 0.2 DEG and 40.7 +- 0.2 DEG. The A-type calcium L-5-methyltetrahydrofolate polymorphism provided in the invention has better solubility and stability and is more beneficial for application in medicines.
US6949512 administering to patient effective amount of lipopolysaccharide binding protein to elevate serum concentration of lipopolysaccharide binding protein in patient to sufficiently high level to suppress lipopolysaccharide induced release of cytokine A therapeutic agent for the treatment of septicemia, its preparation and use, with application in the pharmaceutical industry and medicine. This therapeutic agent contains essential element, the lipopolysaccharide binding protein (LBP). Also disclosed are LBP variants, mutants and hybrid proteins. Murine or rabbit LBP may also be used, besides human LBP.
CN102240288A Application of N-substituted-3,5-dibenzal piperidine-4-one compounds The invention relates to the field of pharmaceutical chemistry, and discloses application of N-substituted-3,5-dibenzal piperidine-4-one compounds with a structure shown in the formula (I) in the preparation of medicaments used for treating breast cancer or ovarian cancer. The compounds have higher inhibitory activity on breast cancer HO8910PM cells and ovarian cancer MDR-MB-231 cells.
WO2013068626A1 Pentacyclic triterpenes for use in the prevention or treatment of acute or subacute myocarditis The use of a pentacyclic triterpene in the production of a pharmaceutical or neutraceutical composition to prevent or to treat a myocardial inflammatory disease, preferably acute or subacute myocarditis, to prevent or to treat a disease involving the appearance of calcium‑salt deposits, and to prevent or to treat a disease involving fibrotic accumulation. Preferably, said pentacyclic triterpene is oleanolic acid. The invention further relates to a pharmaceutical or neutraceutical composition that comprises a triterpene in conjunction with at least one pharmaceutically acceptable adjuvant and/or vehicle or, when the composition is neutraceutical, a neutraceutically acceptable adjuvant and/or vehicle, for treating or preventing a myocardial inflammatory disease, preferably acute or subacute myocarditis, for preventing or treating a disease involving the appearance of calcium‑salt deposits, and for preventing or treating a disease involving fibrotic accumulation. Preferably, said pentacyclic triterpene is oleanolic acid.
CN102552245A Composition containing epigallocatechin gallate and taxol for suppressing tumor cell proliferation The invention belongs to the fields of medicine and gene engineering, and provides a composition for suppressing tumor cell proliferation. The composition for suppressing tumor cell proliferation comprises epigallocatechin gallate and taxol serving as active ingredients, and pharmaceutically-necessary auxiliary materials, wherein the molar ratio of the epigallocatechin gallate to the taxol is 200:1-8:1. As proved by experiments, the treatment effect of taxol on the suppression of tumor cell proliferation can be enhanced remarkably by using the composition prepared from the epigallocatechin gallate and the taxol or using the epigallocatechin gallate during dosing of the taxol. The composition basically has no toxicity on the liver and kidney of a nude mouse, the epigallocatechin gallate inthe active ingredients has rich resources and low price, and the treatment cost of a tumor patient is reduced while the tumor suppression rate is increased simultaneously.
WO2008021486A1 Use of adsborbent carbon microspheres (ast-120) to treat gastroesophogeal reflux disease or symptoms thereof Disclosed herein is the use of adsorbent carbon microspheres (AST-120, MP-146 or kremezin) to treat symptoms of GERD including heartburn, painful swallowing, chest pain, and for reducing bile content in the duodenum. The adsorbent carbon microspheres may be administered alone or in combination with a proton pumb inhibitor.
US7759372 benzimidazole derivatives having antiviral activities, used optionally in combination with a polymerase inhibitor and/or a protease inhibitor A compound of the formula (I): wherein Z4, Z5 and Z9 each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; RA is a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.
CN103211956A External poultice for treating burn The invention relates to the field of pharmaceutical formulas and in particular relates to external poultice for treating burn. The external poultice is characterized by comprising the following raw medicines in parts by weight: 11-14 parts of calcined gypsum, 9-11 parts of felwort, 7-9 parts of gallnut, 6-8 parts of elephant hide, 5-7 parts of Gouania jamnica Miq., 6-8 parts of Paris polyphylla, 3-5 parts of ternate buttercup root, 4-6 parts of folium isatidis, 5-7 parts of cortex moutan, 4-6 parts of lithospermum, 3-5 parts of veronicastrum herb, 4-6 parts of red halloysite, 7-9 parts of paulownia leaf, 6-8 parts of bighead atractylodes rhizome, 1-2 parts of carbonized hair and 8-12 parts of jasmine; and the 16 raw medicines are mixed, uniformly stirred, aired and ground into powder, and the powder is prepared into paste by using sesame oil. The external poultice is low in cost and high in curative effect of treating burn, has no allergic and toxic reaction and side effects, can be used for preventing an allergic reaction and has the effects of removing heat to cool blood, promoting blood circulation to arrest pain, moistening, astringing and the like.
US20050031585 Treating individuals having hepatitis C virus infection, who have failed to respond to therapy with IFN-alpha other than consensus interferon (CIFN), or who, following cessation of therapy with IFN-alpha other than CIFN, have suffered relapse by administering first, then second dosing CIFN, and ribavirin The present invention provides methods for treating individuals having a hepatitis C virus (HCV) infection, which individuals have failed to respond to therapy with an IFN-α other than consensus interferon (CIFN), or who, following cessation of therapy with an IFN-α other than CIFN, have suffered relapse. The methods generally involve a treatment regimen comprising administering a first dosing regimen of CIFN, followed by a second dosing regimen of CIFN. Ribavirin is administered with at least the second dosing regimen.
EP2016048A1 A crystalline form b4 of atorvastatin magnesium and a process thereof Crystalline polymorphic form B4 of Atorvastatin magnesium of figure (1) and processes for its preparation.
US20100029618 Alpha-2 receptor pan agonist and anticonvulsant compositions for treating chronic pain Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an pan-alpha-2 adrenergic receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed.
EP1692123B1 Phenyl-furan compounds as vitamin d receptor modulators The present invention relates to novel, non-secosteroidal, phenyl-furan compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
WO2009010455A3 Pyrazole derivatives as modulators of metabotropic glutamate receptors The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors - subtype 4 ('mGluR4') which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
EP1968575B1 Immunomodulatory pharmaceutical composition containing a combination of three coumarinolignoids The present invention provides a novel pharmaceutical composition consisting of a combination of three coumarinolignoids of formula 1, 2 and 3 isolated from the seeds of the plant Cleome viscosa along with a pharmaceutically acceptable carrier useful as a immunomodulator. The invention also describes the ability of the compounds to modulate humoral and cell mediated immune response. It further provides a process for the preparation of a novel pharmaceutical composition of the said three coumarinolignoids in an optimized ratio to modulate humoral and cell mediated immune response.
CN101041068A Preparation for beauty and for supplementing zinc The invention relates to a composite agent, which uses collagen (or polypeptide) and gluconic acid zinc (or other zinc compound) as material to be mixed and processed. The invention can feed collagen and zinc element to realize beauty treatment, with simple process, low cost, and wide application.
US20090176828 treating pain with minimal cardiovascular and/or sedatory activity side effects;hypertension, depression, glaucoma, elevated intraocular pressure, ischemic neuropathies, optic neuropathy, diabetic retinopathy, stroke, withdrawal symptoms, obsessive compulsive disorder, obesity, diarrhea, nasal congestion Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.
US20110065146 Expression of HIV polypeptides and production of virus-like particles The present invention relates to the efficient expression of HIV polypeptides in a variety of cell types, including, but not limited to, mammalian, insect, and plant cells. Synthetic expression cassettes encoding the HIV Gag-containing polypeptides are described, as are uses of the expression cassettes in applications including DNA immunization, generation of packaging cell lines, and production of Env-, tat- or Gag-containing proteins. The invention provides methods of producing Virus-Like Particles (VLPs), as well as, uses of the VLPs including, but not limited to, vehicles for the presentation of antigens and stimulation of immune response in subjects to whom the VLPs are administered.
CN101108184B Liranaftate complex medicament and method of preparing the same The invention discloses a liranaftate compound drug and its preparation method, which comprises effective dosage of liranaftate and dexamethasone. The preparation method of the invention is: make needed formulation with effective dosage of liranaftate and dexamethasone as well as pharmaceutically allowable dosage of supplementary materials. The effecting speed, curative effect, relapse rate in clinical application and duration for healing of the compound drug far excel that of the liranaftate single drug.
US20070286862 Cancer Associated Antigens The invention relates to isolated nucleic acid sequences which are expressed in cancers, especially gastrointestinal, kidney and prostate cancers, to their protein products and to the use of nucleic acid and protein products for the identification and treatment of cancers.
US20120255045 Inducible small rna expression constructs for targeted gene silencing The invention relates to vectors for the inducible expression of RNA molecules in eukaryotic, particularly mam
US20110021510 Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (mtc) This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiaziniumcompounds”) including Methylhioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: nitrosylation (NOS); nitrosyl reduction (NR); thiosulfonic acid formation (TSAF); oxidative coupling (OC); Cr(VI) reduction (CR); isolation and purification of zwitterionic intermediate (IAPOZI); ring closure (RC); chloride salt-formation (CSF); one of: sulphide treatment (ST); dimethyldithiocarbamate treatment (DT); carbonate treatment (CT); ethylenediaminetetraacetic acid treatment (EDTAT); organic extraction (OE); and recrystallisation (RX). The present invention also pertains to the resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment and diagnosis, etc., for example, for tauopathies, Alzheimer's disease (AD), skin cancer, melanoma, viral diseases, bacterial diseases, or protozoal diseases.
WO2011133879A3 Combination therapies with mitochondrial-targeted anti-tumor agents Described are mitochondria-targeted anti-tumor agents, death receptor agonists, autophagy inhibitors, and NF-ĸB signaling pathway inhibitors, and methods of making and using the same for the treatment of disorders associated with unwanted cell proliferation.
CN1927220A Montmorillonite gelling preparation for treating diarrhea and gastritis and its preparation process The invention relates to a montmorillonite gel agent for treating loose bowel movement and gastritis, and relative production. Wherein, said gel agnet is formed by 180-220 deals of montmorillonite, 0.15-150 deals of corrigents, 0.1-5 deals of conservatives and 640-810 deals of deionized waters, to be dispersed by ultrasonic wave, to form uniform gel. And the production comprises that (1) weighting montmorillonite, corrigents, conservatives and deionized waters; (2) adding montmorillonite into deionized water to be mixed uniformly, then adding corrigents, conservatives, to be mixed for 20min or 2 hours; (3) treating the uniform mixture with ultrasonic wave into uniform gel; (4) disinfecting and packing the gel. The inventive gel agent has simple application and better effect.
US20120100234 Non-occluding nasal moisturizer and methods of use Compositions are provided that provide improved nasal moisture, clarity, and lubrication. Compositions are oil-in-glycerin emulsions that include a surfactant promoting emulsification of a hydrophobic or otherwise water insoluble bioactive agent. The compositions are used in methods of promoting improved nasal moisture and reduction in nasal congestion.
US20080176841 (amidomethyl-amido)-(carboxy/amido)epoxide derivatives; cathepsin inhibitor; antiinflammatory, anticarcinogenic, antidiabeticagent, antiallergen, autoimmune and neurodegenerative disorders Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
CN101940793B Hydroxypropyl-beta-cyclodextrin clathrate compound of cantharidin and cantharis extractive and preparation method thereof The invention discloses a hydroxypropyl-beta-cyclodextrin clathrate compound of a cantharidin and cantharis extractive and a preparation method thereof. The concrete method comprises the following steps of: precisely weighing cantharidin and hydroxypropyl-beta-cyclodextrin according to the molar ratio; adding 10-30ml of 60-80 percent alcohol; stirring for 1-3 hours at the rotating speed of 90-120r/min and the constant temperature of 30-50 DEG C; filtering through a 0.22mum microporous filter membrane; collecting filter liquor; and drying for 3-5 hours at the temperature of 60 DEG C to obtain the clathrate compound. The hydroxypropyl-beta-cyclodextrin clathrate compound of the cantharidin and cantharis extractive can obviously increase the solubility of drugs and reduces the mucous membrane thrill of the cantharidin and cantharis extractive.
CN101816679A Film-forming type iodine disinfectant and preparation method thereof The invention relates to disinfectants, in particular to a film-forming type iodine disinfectant and a preparation method thereof. The film-forming type iodine disinfectant comprises the following components in percentage by weight: 0.045 to 0.055 percent of iodine, 0.045 to 0.055 percent of potassium iodide, 0.45 to 0.50 percent of chlorhexidine acetate, 12.0 to 15.0 percent of polyvinyl alcohol, 0.5 to 2.0 percent of benzyl alcohol, and the balance of purified water. The method for preparing the film-forming type iodine disinfectant comprises the following steps of: firstly, adding a properamount of the purified water into the iodine and potassium iodide, and stirring and dissolving to obtain solution of iodine and potassium iodide according to the content and components; secondly, dissolving the chlorhexidine acetate and benzyl alcohol by using the purified water with the temperature of 50 DEG C in another container, adding the polyvinyl alcohol, and stirring and mixing uniformly;and finally, adding the solution of iodine and potassium iodide, and stirring and mixing uniformly. The film-forming type iodine disinfectant can be applied to multiple wound disinfection treatment for human bodies.
CN101555291A Extraction and separation technology of ginseng polysaccharides The invention relates to an extraction and separation technology of ginseng polysaccharides. The main quality characteristics thereof are as follows: the protein is detected as negative, the water solubility performance can achieve 100 percent, and the content of galacturonic acid is 10.0 percent-30.0 percent.
WO2010011856A2 Stereospecificity of methylsulfinyl reduction This disclosure relates to compositions and methods of use involving compounds (e.g., drugs) containing methylsulfinyl moieties. For example, a compound may be administered in an excess of either the R- or S-epimer of the methylsulfinyl moiety based on whether the compound exhibits higher biological activity when the methylsulfinyl moiety is present in the methylsulfinyl-oxidized form or the methylsulfide-reduced form.
WO2007065924A1 Bicyclic hξteroyclic compounds as antiinflammatory agents There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, A, D, X, W, m and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.
CN101229193A External Chinese patent medicine for treating skin ulceration and organism gangrene The invention discloses a Chinese patent medicine for external use, in particular to an externally used Chinese patent medicine used for treating skin ulceration and organism gangrene, belonging to the externally used medicine technology field; the invention is characterized in that the invention is prepared with the following medicine materials by weight portion, cinnabar of 0.5 to 1 portion, ice of 2 to 4 portions, pearl of 7 to 10 portions; the invention has the effects of antisepsis and anti-inflammation, facilitating the growth of tissue and muscle and promoting the regeneration of epidermal cells. The invention is the ideal externally used Chinese patent medicine for curing skin ulceration, in particular to organism gangrene.
US7045152 Pulmonary disorders in which the S-nitrosoglutathione(GSNO) pool or glutathione pool in the lung is depleted and where reactive oxygen species in lung are increased, are treated by delivering into the lung an agent causing repletion of GSNO Pulmonary disorders in which the GSNO pool or glutathione pool in the lung is depleted and where reactive oxygen species in lung are increased, are treated by delivering into the lung as a gas, agent causing repletion or increase of the GSNO pool or protection against toxicity and does so independently of reaction with oxygen. Agents include ethyl nitrite, NOCl, NOBr, NOF, NOCN, N2O3, HNO, and H2S. Optionally, N-acetylcysteine, ascorbate, H2S or HNO is administered in addition to other GSNO repleting agent to potentiate the effect of said agent.
CN103006601A Orlistat tablet and preparation method thereof The invention discloses an orlistat-containing tablet and a preparation method thereof. The orlistat-containing tablet is prepared by directly tabletting a silicon dioxide-containing orlistat phospholipid composition and pharmaceutic adjuvants, wherein the weight ratio of orlistat to phospholipid to silicon dioxide which are contained in the silicon dioxide-containing orlistat phospholipid composition is 1:(0.5-1.5): (0.5-3). The orlistat-containing tablet disclosed by the invention solves the problems of tabletting sticking and poor storage stability of the conventional process of the orlistat and enhances the in-vivo dissolvability of the orlistat.
CN1751683A Skeleton type slow-releasing tablets contg. lycopodine-A and its derivatives or its salts and preparing process thereof A skeleton-type slow-releasing tablet of huperzine A or its derivative or its salt is prepared from huperzine A or its derivative or its salt, the hydrophilic gel as skeleton slow-releasing material (20-90 Wt%) and filler (5-75 Wt%). Its preparing process is also disclosed. Its advantages are high slow-release effect (12 hr) and curative effect.
WO2011016459A1 Thienooxazepine derivative Disclosed is a compound which has serotonin 5-HT2C receptor activating activity. Specifically disclosed is a compound represented by formula (I) or a salt thereof. (In the formula, the symbols are as defined in the description.)
WO2010058333A1 Lactams as beta secretase inhibitors Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment methods of synthesis, and intermediates are also disclosed.
CN101721631A Hotly-compressed medicine bag for hyperosteogeny The invention relates to a hotly-compressed medicine bag for hyperosteogeny, which contains 30 grams of notopterygium root, 30 grams of pubescent angelica root, 15 grams of mastic, 15 grams of myrrh, 30 grams of lycopodium clavatum, 30 grams of garden balsam stem, 15 grams of dahurian angelica root, 15 grams of wild ginger, 30 grams of great burdock fruit, 30 grams of white mustard seed, 30 grams of chastetree fruit, 15 grams of rhizoma typhonii, 30 grams of giant mistletoe, 45 grams of radix clematidis, 30 grams of jobstears, 60 grams of licorice, 15 grams of radix sileris and 10 grams of safflower. When in use, a little vinegar is added into the medicine bag, and the medicine bag is put into a kettle for braising for half an hour and then is hotly compressed at a focus. The invention has unique formula, simple preparation, convenient use, low cost, short treatment course, quick acting and high cure rate.
US7157457 Compounds useful in the treatment of inflammatory diseases There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
CN102497857A Nanostructured sildenafil base, its pharmaceutically acceptable salts and co-crystals, compositions of them, process for the preparation thereof and pharmaceutical compositions containing them The present invention is directed to nanostructured (nanoparticulated) Sildenafil base, its pharmaceutically acceptable salts and co-crystals, compositions containing them, process for the preparation thereof and pharmaceutical compositions containing them. The nanoparticles of Sildenafil base, its pharmaceutically acceptable salts and co-crystals, compositions containing them according to the invention have an average particle size of less than about 500 nm. Sildenafil citrate is inhibiting cGMP specific phosphodiesterase type 5 (PDEV), an enzyme that regulates blood flow in the penis. The compositions of the invention are useful in the treatment of male or female sexual dysfunction and pulmonary arterial hypertension (PAH).
US20090258903 Aminoethane Sulfonamide Orexin Receptor Antagonists The present invention is directed to aminoethane sulfonamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
US20120122882 Substituted Pyrrolo-Pyrimidine Derivatives, Process for Their Preparation and Their Use as Kinase Inhibitors Substituted pyrrolo-pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.
US20110046224 Methods to accelerate muscle development, decrease fat deposits, and enhance feeding efficiency in pigs A natural method to promote or enhance food efficiency and muscle/fat ratio in animals is described, particularly for pigs, through the administration of an effective amount of pure ferulic acid, substantially pure ferulic acid or ferulic acid formulations. Prepared food and formulations for animals are also described, which can increase muscular development in pigs, decreasing fat deposits or promoting or increasing animal growth or enhancing food efficiency in an animal. Effective amounts of pure ferulic acid or substantially pure ferulic acid use in said food preparations and formulations are described.
WO2008001878A1 Hydroxy ether compound, process for production of the compound, and use of the compound Disclosed is a substance having a high antibacterial activity in a wide variety of systems and excellent in safety, stability, feeling of use and usability. Specifically, disclosed is a hydroxy ether compound represented by the general formula (1): (1) wherein R1 represents a hydrogen atom or a methyl group; R2 and R3 independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms or an alkenyl group having 2 to 8 carbon atoms, or R2 and R3, together with a carbon atom to which R2 and R3 are bound, form an aliphatic cyclic hydrocarbon group, provided that the sum total of the carbon atoms of R2 and R3 ranges from 2 to 8; and n is 1 or 2.
EP1211305B1 Fat compositions Fat compositions containing from 0.1 to 59.8% by weight of triglycerides, from 40 to 99.7 % by weight of diglycerides, from 0.1 to 10 % by weight of monoglycerides and 5 % by weight or less of free fatty acids, wherein, in the acyl constituting the diglycerides, the content of φ3-unsaturated acyl having 20 or more carbon atoms amounts to 15 to 89.5 % by weight and the content of monoenacyl amounts to 10 to 84.5 % by weight; and medicinal compositions for oral administration and foods containing these fat compositions. The above fat compositions can effectively exhibit the physiological functions (inhibiting platelet agglutination, etc.) inherent to the φ3-unsaturated fatty acids, show an excellent effect of promoting body fat burning, are excellent in stability against oxidation, flavor, etc. and have high fluidity.
DE102013000700A1 Composition useful e.g. for treating inflammatory diseases of oral and pharyngeal cavity, comprises virustatic and/or antiviral polysaccharide, surface disinfectant, optionally acidic glycosaminoglycan and optionally local anesthetic Composition in a solid or liquid form, preferably solid dosage form, comprises: (a) 0.1-40 wt.%, preferably 3-18 wt.% at least one polysaccharide, preferably a virustatic and/or antiviral polysaccharide; (b) 0.001-5 wt.%, preferably 0.05-0.5 wt.% at least a surface disinfectant; and (c) 0.01-10 wt.%, preferably 0.1-2 wt.% optionally at least one acidic glycosaminoglycan or its salts or derivatives, preferably hyaluronic acid or its salts; (d) 0.01-5 wt.%, preferably 0.1-1 wt.% optionally at least one local anesthetic. ACTIVITY : Antiinflammatory. The antiinflammatory activity of the composition was tested in patients (18-75 years old) with inflammatory diseases of the ear and throat by administering composition (lozenge tablet containing 0.25 wt.% glycerin, 10 wt.% carrageenan, 0.25 wt.% polyhexanide, 77.41 wt.% matrix former, 11.75 wt.% carrier substance, and 0.34 wt.% flavored component) for 3 days. The result showed that the lozenge tablet exhibited reduction of inflammation (1.8) (according to the school grading system), compared to the tablets (mono preparation of active ingredients) (3.0). MECHANISM OF ACTION : None given.
CN103520180A Medicine composition for treating eczema, seborrheic dermatitis and psoriasis and preparation method thereof The invention provides a medicine composition for treating eczema, seborrheic dermatitis and psoriasis and a preparation method thereof and belongs to the field of medicines. The problems of the existing medicine for treating eczema, seborrheic dermatitis and psoriasis that the disease is easy to relapse after the medicine is not orally taken any more, the curing rate is low and the treatment course is relatively long are solved. The medicine composition is prepared from fluocinonide, paeonol and emulsion matrix. The invention also provides a preparation method of the medicine composition for treating eczema, seborrheic dermatitis and psoriasis. According to the medicine composition, fluocinonide and paeonol are combined to prepare emulsifiable paste, so that the medicine composition has the obvious curative effect in treatment of eczema, seborrheic dermatitis and psoriasis; moreover, the disease is difficultly relapsed and the poor reaction is reduced; the medicine composition is short in treatment course.
CN103054894A Application of Phyllanthus urinaria polysaccharide in preparation of anti-hepatitis B virus medicines The invention discloses an application of a Phyllanthus urinaria polysaccharide PUIP III in the preparation of anti-hepatitis B virus medicines. The Phyllanthus urinaria polysaccharide PUIP III is composed of rhamnose, arabinose, mannose and glucose, the molar ratio of rhamnose to arabinose to mannose to glucose is 0.27:0.28:0.1:0.35, and the molecular weight of the Phyllanthus urinaria polysaccharide is 418793.5. The Phyllanthus urinaria polysaccharide is obtained through artificially extracting the medicinal plant Phyllanthus urinaria, separating and purifying. In-vitro biological activity experiments show that the PUIP III can inhibit the HBsAg and HBeAg secretion and the HBV-DNA duplication in the HepG2.2.2.15 cell culture, and has a certain in-vitro anti-HBV activity; and in-vivo activity experiments show that the PUIP III has an obvious inhibition effect on DHBVDNA in ducks, has small rebound, and can be used for preparing the anti-hepatitis B virus medicines and liver protection healthcare products.
CN101112448B Donkey-hide gelatin composition having immunity improving effect and method of making the same The present invention discloses a composition to enhance immunity and the preparation method. The combination is prepared by of donkey-hide glue, hawthorn, ginseng, largehead atractylodes rhizome, pilose Asiabell root and radix rehmanniae preparata. The excipients can be added into the composition of the present invention according to the conventional process to prepare the tablets, capsules, oral liquor, granules and other formulations. The composition of the present invention can greatly improve the immunity, the formulation is designed with easy administration and better action of the effects; the formulation of the present invention has better taste and taste feeling, which can increase the compliance of the patients and have simple preparation process and strong maneuverability.
EP1935415A2 Treatment of androgen-deprivation induced osteoporosis The present invention provides methods for reducing the incidence of inhibiting, suppressing, and treating androgen-deprivation induced osteoporosis, bone fractures and/or loss of bone mineral density (BMD) in men having prostate cancer, comprising administering to a male human subject having prostate cancer a toremifene and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide or any combination thereof. The present invention also provides methods of treating, preventing, suppressing, inhibiting, or reducing the incidence of hot flashes, gynecomastia, and/or hair loss in a subject, comprising same.
CN101439064A Nourishing tonic for sport The invention relates to a sports nutritional supplement, the main components of which include acanthopanax extract and octocosanol. The sports nutritional supplement has the functions of promoting hepatin synthesizing, increasing resistance and recovering physical fitness and is particularly suitable for athletes.
WO2013123444A1 Sulfonyl compounds that interact with glucokinase regulatory protein The present invention relates to sulfonyl compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
US7501124 Administering allogenic or xenogeneric cell; complexing with antigen Methods for inducing T cell tolerance to a tissue or organ graft in a transplant recipeint are disclosed. The methods involve administering to a subject: 1) an allogeneic or xenogeneic cell which expresses donor antigens and which has a ligand on the cell surface which interacts with a receptor on the surface of a recipient T cell which mediates contact-dependent helper effector function; and 2) an antagonist of the receptor which inhibits interaction of the ligand with the receptor. In a preferred embodiment, the allogeneic or xenogeneic cell is a B cell, preferably a resting B cell, and the molecule on the surface of the T cell which mediates contact-dependent helper effector function is gp39. A preferred gp39 antagonist is an anti-gp39 antibody. The allogeneic or xenogeneic cell and the gp39 antagonist are typically administered to a transplant recipient prior to transplantation of the tissue or organ. The methods of the invention can be used to induce T cell tolerance to transplants such as liver, kidney, heart, lung, skin, muscle, neuronal tissue, stomach and intestine. A method for treating diabetes comprising administering to a subject allogeneic or xenogeneic cells expressing donor antigens, a gp39 antagonist and pancreatic islets is also disclosed.
WO2011075958A1 Use of toll-like receptor-3 agonist in the preparation of medicament for promoting wound healing The present invention discloses the use of a toll-like receptor-3 (TLR3) agonist in the preparation of medicament for promoting wound healing. A toll-like receptor-3 (TLR3) agonist, particularly polyriboinosinic polyribocytidylic acid, can promote wound healing and be used as the active ingredient of medicament for promoting wound healing.
EP2396029A1 Antibiotic therapy to reduce the likelihood of developing post-infectious irritable bowel syndrome The present invention provides for methods of preventing IBS, preventing long term irregular bowel pattern, reducing the likelihood of developing or having IBS, reducing the likelihood of developing or having long term irregular bowel pattern, mitigating IBS, mitigating long term irregular bowel pattern and reducing the likelihood of developing non-ulcer dyspepsia. The methods comprise providing an antibiotic and administering the antibiotic to a subject in need thereof.
WO2005054250A1 Tricyclacetalactonin, Preparation and Use there of The invention relates to tricyclacetalactonin, preparation and use there of. Said tricyclacetalactonin is prepared from Streptomyces albogriseolus of A2-2002. As being proved by the experiments, said compounds can be used as cell cycle inhibitor, apoptosis inducer or antitumor agent.
US20080096852 Use of oculosurface selective glucocorticoid in the treatment of dry eye Topical ophthalmic compositions and methods for treating dry eye are described. The compositions and methods of the invention are based on the finding that the oculosurface selective properties of the glucocorticoid rimexolone make this anti-inflammatory agent particularly well-suited for treating dry eye. As a result of the limited ability of rimexolone to penetrate the cornea, a high portion of the drug remains on the surface of the eye, which is the primary locus of the inflammatory conditions associated with dry eye. This enables a very low concentration of drug to be utilized, which in turn reduces the potential for elevations of intraocular pressure and cataract formation.
US20080318930 Sulfonyl Compound as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase-1 Sulfonyl derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome or Syndrome X, and other symptoms associated with NIDDM.
CN101475583B Dibutyl tin dichloride schiff alkali coordination compound, as well as preparation method and application thereof The invention discloses a dibutyltin dichloride Schiff base complex of a structural formula on the right. The preparation method of the complex comprises: adding 2.5 to 3.0mmol of 2- hydroxyl 1-naphthaldehyde p-hydroxybenzohydrazide, 5.0 to 8.0mmol of sodium alcoholate and 50 to 100mL methanol into a round bottom flask, stirring the mixture for 0.5 to 2h, and adding 2.5 to 3.5mmol dibutyltin dichloride and heating for reflux for 5 to 8 hours with stirring; and cooling and filtering the solution, evaporating the filtrate to dryness by using a rotary evaporator and obtaining yellow solid, and recrystallizing the yellow solid by using methylene dichloride-ethanol and obtaining orange crystals. The complex has higher anticancer activity and can be used as a raw material for preparing drugs for treating gastric cancer, nasopharyngeal darcinoma, human liver cancer or leukemia. Compared with the prior widely used platinum-based anticancer materials, the complex has the characteristics of high anticancer activity, excellent lipid solubility, low cost, simple preparation methods and the like and provides a new way for developing anticancer drugs.
US20090105088 Mutant bank The invention relates to a mutant bank of diploid micro-organisms which consists of a population of mutant cells in which at least one cell has a random mutation which disrupts the activity of at least one gene, wherein the micro-organism is inducible into haploid form. The invention further relates to a method of using the mutant bank to identify the genes which contribute to a chosen phenotype.
US7019021 such as 2-(6-bromo-3-dimethylamino-2-methylphenylimino)imidazolidine; stress Compounds of the formula (II) wherein R1, R2, R3, R4, and R5 are as set forth herein, pharmaceutical compositions containing them, and their use in treating urinary incontinence.
WO2012090218A1 Synergistic effects of the combination of the specific compounds with paracetamol and their effects on various diseases This invention is based on efficacy of compounds and combination of compounds. Which essential for treatment of a number of diseases. These are pain, antiinfilamation, hepatoprotective, fever, allergy thereof. This combination has less toxicity, it has highly hepatotoxicity. The main mechanism of action of paracetamol is considered to be the inhibition of cyclooxygenase (COX) that it is highly selective for COX-2. The concentration of paracetamol is 500mg and thereof. Racemethionine is anti-oxidant nutritional supplement to treat liver diseases caused by alcoholism including cirrhosis. It acts as important sulphur and methyl group donor in detoxification reactions in liver cells. The concentration of racemethionine is 50mg and thereof. All effective cold remedies containing phenylephrine. The concentration of Phenylephrine is 5 mg/tablet and thereof. Phenylephrine to form an allergy medication with both antihistamine and decongestant properties. Chlorphenaminemaleate is suitable compound for cough and cold.chlorphenamine maleate to form an allergy medication with both antihistamine and decongestant properties. The concentration of chlorphenaminemaleate is 2 mg/tablet and thereof. Caffeine may also have hepatoprotective properties. Increased caffeine consumption is associated with less severe liver injury among those at high risk for liver disease, such as those with alcoholism, obesity, or hemochromatosis. The concentration of caffeine is 15 mg/tablet and thereof.
US20080227727 Administering topoisomerase inhibitor (such as camptothecin, irinotecan, topotecan, doxorubicin, teniposide, etoposide ) and E3 ubiquitin ligase inhibitor 2-(4-vinylpyridynyl)1,3-diacyl/thiocarbonyl indene derivative for modulating cell growth Disclosed are methods and compositions useful in identifying an E3 ubiquitin ligase inhibitor and modulating cell growth, comprising contacting a cell with an effective amount of an inhibitor of an E3 ubiquitin ligase, and contacting the cell with an effective amount of a topoisomerase inhibitor, wherein the treatment with the E3 ubiquitin ligase inhibitor and topoisomerase inhibitor modulates cell growth in comparison to a cell treated with the topoisomerase inhibitor alone. The present invention further provides methods for identifying and making an E3 ubiquitin ligase inhibitor.
EP2776565A1 Methods and compositions for treating diseases, disorders or injury of the nervous system Disclosed herein are compositions and methods of use thereof for treating diseases, disorders and injuries of the nervous system, com¬ prising a combination of a RTP801 or RTP801L inhibitor, and a Casp2 inhibitor.
US20120245166 Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.
CN102525879A Method for preparing aprepitant solid dispersing composition The invention belongs to the field of medicament preparations, and in particular provides a method for preparing an aprepitant solid dispersing composition. The composition contains aprepitant and at least one water-soluble polymer. The method comprises the following steps of: crushing, mixing, melting and extruding the aprepitant and the water-soluble polymer in an extruder, wherein the heating temperature of the extruder is not below the Tg value of the water-soluble polymer or between 30 DEG C below the melting point and the melting point of the aprepitant; and cooling and curing the extruded product, and thus obtaining the solid dispersing composition. The aprepitant solid dispersing composition prepared by the method is dissolved in a water-based medium on an unexpected high level in relatively short time, and has improved dissolving characteristic and remarkable physical stability.
US20120251521 Technical field and industrial applicability of the invention The present invention is a solution or colloid of fullerene, SWNTs, or graphene in cyclic terpenes, lactones, terpene-alcohol, fatty-acid alcohols, and lactones following ultrasonication and ultracentrifugation processing, for oil-energy, biological, electrical-thermal applications. The compositions are useful as fuel/oil/grease/gels (synthetic included), oil/fuel/additives/propellants, identification dyes, and heat-transfer fluids. Other functions are phase-change fluids for solar energy power plants, antifreeze, electronic dyes, electrolytic fluid/solvent, electrically-thermally conductive material for electrochemical, dielectric, filler/adhesive for semiconductor, eletro-optical, and liquid crystal substrates/coatings for touch sensitive transmissive or reflective displays. When combined with gelatin the formulations can function as dichroic-optical coatings for thin-films/waveguides/holograms. Such formulations may also be used as photovoltaic paint, electrorheological, thermophoretic-thermodiffusion, electrohydrodynamics, electric propulsion, laser enhancement, plasma jets, and magnetohydrodynamics. Energy use includes high-temperature superconductivity, or hydrogen storage using carbon, alumina, or silica supported Pd, Pt, or Zn catalysts. Biological applications include anticancer, antiviral, antifungal, drug delivery, skin permeable agents, and lubricant use.
CN1784994A Method for preparing sour milk contg. micron ginseng, antler, pearl, and pollen pini for tonifying-Yang, dispelling-fatigue and enriching-calcium A micron-class health-care sour milk for invigorating Yang, relieving fatigue and supplementing Ca is prepared from traditional milk, micron-particles of ginseng, antler, pine pollen and pear, oligose and useful intestinal bacteria through proportional mixing, processing and fermenting. Its advantages are high effect and rich nutrients including vitamins, minerals, etc.
CN101269064A Application of myricetin in medicament for treating prostate gland disease The invention discloses the application of myricetin in the treatment of prostatic hyperplasia and/or prostatitis diseases. The prepared drug can contain only myricetin or the compound of myricetin. The prepared drug can be prepared into common tablets or capsules, slow-release tablets or capsules as well as injections and suspensions.
WO2008119543A1 Polymorph of clarithromycin (form v) The invention relates to a polymorphous form of clarithromycin (form V) as well as the production and use thereof.
CN102949754A Uterine cavity hemostasis anti-adhersion temperature-sensitive gel and preparation method thereof The invention provides a uterine cavity hemostasis anti-adhersion temperature-sensitive gel and a preparation method thereof, and relates to a postoperative anti-adhesion gel and a preparation method thereof. The uterine cavity hemostasis anti-adhersion temperature-sensitive gel comprises the following materials in percentage by weight: 1-4% of carboxymenthyl chitosan, 17-45% of poloxamer F127, 5-20% of glycerol and the balance of purified water. The preparation method comprises the following steps: dissolving the carboxymenthyl chitosan and poloxamer F127 into warm water and cold water respectively, mixing the two solutions into glycerol, complementing water to sufficient quantity, stirring evenly, standing and defoaming in a refrigerator to obtain a colorless and transparent solution, filtering the solution with a 300-mesh sieve, sub-packaging the filtrate into a uterine perfusion device, sterilizing through cobalt-60, and storing in a refrigerating chamber for later use. The uterine cavity hemostasis anti-adhersion temperature-sensitive gel is of a medical material which is good in biocompatibility, safe, non-toxic and non-irritant, has the effects of stopping bleeding and prompting cure of wound surfaces while being anti-adhesion, thereby being more suitable for the demand of cure of clinical wound surfaces.
US7091187 Using steroid; autoimmune disease The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, S represents a steroid subunit (steroid moiety) derived from steroid drug with anti-inflammatory activity and L represents a linker molecule linking M and S, (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory diseases and conditions in humans and animals. Such compounds inhibit many cytokines and immune mediators involved in immune responses which cause inflammation, allergy, or alloimmunity, including without limitation IL-1, 2, 4, 5, 6, 10, 12, GMCSF, ICAM, and TNF-α. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.
CN101687854A Compounds and compositions as C-KIT and PDGFR kinase inhibitors The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRa and PDGFRss kinases.
WO2013085352A1 Pharmaceutical composition comprising diaminodiphenylsulfone or the pharmaceutically acceptable salts thereof for preventing or treating diseases associated with decrease in bone mass The present invention relates to a pharmaceutical composition comprising diaminodiphenylsulfone (dapsone, DDS) or the pharmaceutically acceptable salts thereof as active ingredients for preventing or treating diseases associated with a decrease in bone mass. The composition according to the present invention may effectively enable losses in bone density and bone mass to be recovered, and therefore can be effectively used in preventing or treating diseases associated with a decrease in bone mass such as osteopenia or osteoporosis.
WO2014136075A1 H3 antagonists containing phenoxypiperidine core structure The present invention relates to new histamine H 3(H 3) receptor subtype selective ligands of the general formula (I) and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/ or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and the use of these compounds as medicaments for treatment and/or prevention of conditions which require modulation of H 3receptors. The invention also cover the combinations of a compound of the general formula (I) and an acetylcholinesterase inhibitor.
US20110189165 Method of identifying disease risk factors Provided herein is a method for identifying a genetic variant that is associated with development of a condition of interest (e.g., Alzheimer's disease), and genetic variants so identified. Methods of treatment with an active agent (e.g., with a particular active agent and/or at an earlier age) is also provided, upon detecting a genetic variant described herein. In some embodiments, the genetic variant is a deletion/insertion polymorphism (DIP) of the TOMM40 gene. Kits for determining if a subject is at increased risk of developing late onset Alzheimer's disease is also provided. Kits for determining if a subject is responsive to treatment for a condition of interest with an active agent are further provided.
WO2014028968A1 Perforin inhibiting benzenesulfonamide compounds, preparation and uses thereof Compounds of formula (la) and pharmaceutically acceptable salts, solvates, and hydrates thereof and related methods of modulatin perforin activity on a cell: wherein Ring A is selected from a 6-10 membered aryl, 5-6 membered cycloalkyi, 5-6 membered heteroaryl or 5-6 membered heterocyclyl, wherein the heteroaryl and heterocyclyl rings comprise at least one heteroatom selected from N, O or S; and wherein the aryl, cycloalkyi, heteroaryl or heterocyclyl rings are optionally substituted with 1 to 3 substituents selected from halo, nitro, -C1-Cealkyl, -C1-Ceaminoalkyl, -C1-C6hydroxyalkyl, -haloC1-C6alkyl, -C1- C6alkoxyl, -haloC1-C4)}-[alpha-L-rhamnopyranosyl (1->2)]-3-O-beta-D-glucopyranoside preparation method and an application for inhibiting angiogenesis thereof; the preparation method is composed of extracting polyphylla by using organic solvent and preparing chonglou saponin I by silica gel and reverse phase silica gel chromatography which can be used as an anti-neoplastic drug.
CA2506492A1 Irrigation solution for use in ultrasound energy assisted surgery The invention provides a biocompatible, injectable sterile aqueous solution for use in high-intensity-ultrasound-energy-assisted surgery comprising antioxidants elected from the group consisting of ascorbic acid, glutathione and mixtures thereof an a buffered biocompatible solution for the reduction and limitation of reactive oxygen species.
US20120282341 Lipid Formulated Compositions And Methods For Inhibiting Expression Of Eg5 And VEGF Genes This invention relates to compositions containing double-stranded ribonucleic acid (dsRNA) in a SNALP formulation, methods of using the compositions to inhibit the expression of the Eg5/KSP and VEGF, and methods of using the compositions to treat pathological processes mediated by Eg5/KSP and VEGF expression, such as cancer.
WO2006123644A1 Int6 PROTEIN INVOLVED IN HYPOXIA STRESS INDUCTION AND USE THEREOF As a factor involved in hypoxia stress induction that enhances vasculaliation, Int6 is now identified successfully which is capable of binding to an HIF2α binding factor. It is found that Int6 can inhibit the transcription of an HIF2α hypoxia stress-inducible gene through the interaction between Int6 and HIF2α. A substance capable of inhibiting the expression or function of Int6 can enhance a promoting effect on the transcription of an HIF2α hypoxia stress-inducible gene to promote the vasculaliation, and therefore is expected to show a therapeutic effect on various vascular diseases such as myocardial infarction.
CN102603678A Diphenyl-methyl piperazine compound, preparation and use of the diphenyl-methyl piperazine compound The invention relates to a diphenyl-methyl piperazine compound as shown in a formula I, a preparation method and a use of the diphenyl-methyl piperazine compound. The compound acts on an antagonist of a peripheral cannabinoid-1 (CB1) receptor, so the compound is applicable to treating, preventing and inhibiting diseases mediated by the CB1 receptor, specifically applicable to treating obesity and the diseases related to the obesity.
CA2345064C Fentanyl composition for the treatment of acute pain A pharmaceutical composition for the treatment of acute pain by sublingual administration is described. The composition comprises an essentially water-free, ordered mixture of fentanyl or a pharmaceutically acceptable salt thereof in the form of microparticles which are adhered to the surface of carrier particles which are substantially larger than the particles of fentanyl, and are essentially water-soluble. In a preferred embodiment, the composition also contains a bioadhesion and/or mucoadhesion promoting agent. The invention also relates to the preparation of the composition, and to the use of the composition for the treatment of acute pain.
US20110092563 Statin and omega-3 fatty acids for lipid therapy A method of lipid therapy, comprising providing a subject group having a baseline triglyceride level of 200 to 499 mg/dl and being at or near its low-density lipoprotein cholesterol (LDL-C) level goal, and reducing the triglyceride level and the non-high-density lipoprotein cholesterol (non-HDL-C) level of the subject group as compared to treatment with a 3-hydroxy-3-methyl glutaryl coenzyme A (HMG CoA) inhibitor alone, by administering to the subject group an effective amount of an HMG CoA inhibitor and a composition comprising omega-3 fatty acids.
EP1727820B1 Amine derivatives with tyrosinkinase inhibiting activity Compounds of formula (I), wherein R1, R2, R3, R4, R5, B and X have the meanings cited in Claim 1, are inhibitors of tyrosine kinases, particularly TIE-2, and Raf kinases and can be used inter alia in the treatment of tumors.
CN103040832A Application of substituted cyanobenzene in preparation of fungal infection resisting drugs The invention relates to application of substituted cyanobenzene in preparation of fungal infection resisting drugs and particularly discloses a substituted cyanobenzene compound 3-[4-(4-cyanobenzyl)-piperazin-1-yl]-methyl-6-(2-bromo-4,5-dimethoxyphenyl)-2H-pyran-2-one or pharmaceutically acceptable salts thereof and a preparation method and medicinal application thereof. The in-vitro fungal growth inhibition activity of the compound is determined through a micro-dosage liquid-based dilution method; and shown by experimental results, the 80% inhibition concentration of the substituted pyranone compound to the growth inhibition of candida albicans is 125 micrograms/milliliter. Shown by pharmacodynamic results, the compound or pharmaceutically acceptable salts thereof can be expected to be applied to drugs for prevention and treatment of diseases caused by fungal infection.
DE102006002816A1 Agent, useful for the therapy and prophylaxis of human immunodeficiency virus, and as a food supplement, comprises zeolite and further materials Agent (I) for the therapy and prophylaxis of HIV comprises zeolite and optionally further materials. - ACTIVITY : Anti-HIV. - MECHANISM OF ACTION : None given.
CN101406511A External-use medicament for treating vitiligo The invention discloses an external applied medicine for treating vitiligo. The formula for the medicine is prepared by the following medicine formula in portion by weight: 20 portions of malaytea scurfpea, 18 portions of semen astragali complanati caltrop, 18 portions of chaulmoogra, 18 portions of litharge, 10 portions of mercurous chloride, 18 portions of fructus cnidii and 6 portions of lopseed. The external applied medicine has the advantages that vitiligo is difficult to relapse after being healed, and the external applied medicine has no stimulant function; slight patients can be healed after 1 to 2 treatment periods, and heavy patients can be healed after 3 to 5 treatment periods; and the effective rate is 76 percent, and the cure rate is 62 percent.
CN101190219A Phthalyl sulfathiazol tablet chewable tablets for dog or cat The invention discloses a phthalylsulfathiazole-tablet chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the existing tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 10 to 30 percent of phthalylsulfathiazole-tablet.
CN1957937B Dispersion tablet of Glucurolactone, and preparation method A dispersing tablet of glucuronolactone is prepared from glucuronolactone (30-80 wt. %) and medical assistant (20-70wt. %) chosen from disintegrant, filler, wet adhesive and lubricant. Its preparing process is also disclosed.
US20100055205 Functional consumable compositions for promoting skin health and methods for using the same A functional consumable composition for promoting skin health may comprise, for each 100% by dry weight, no more than about 0.2% by dry weight catechin and no more than about 2% by dry weight amino acid. The amino acid may comprise at least one of 1-proline and 1-arginine, and the weight % 1-proline to weight % 1-arginine may be greater than about 2. Another functional consumable composition may comprise no more than about 0.2% by dry weight catechin and at least one of lipoic acid, selenium, vitamin E, vitamin B, and vitamin C. A source of the catechin may comprise at least one of white tea solids and epigallocatechin gallate extract. Methods for using such functional consumable compositions are also described.
CN102225168A Mongolian medicine for treating pharyngitis The invention relates to a medicament, namely, a Mongolian medicine for treating pharyngitis. The Mongolian medicine is prepared from the following bulk medicaments in parts by weight: 5-9 parts of clove, 2-3 parts of concretio silicea bambusae, 8-12 parts of licorice root, 8-12 parts of costustoot, 8-12 parts of myrobalan, 8-12 parts of fragrant plantain lily flower and 0.3-0.7 part of borneol. The Mongolian medicine has the beneficial effects of short treatment course, rapid action and no toxic effect for pharyngitis and also has the characteristics of available materials, low cost, wide applying range and the like, and is simple to prepare and convenient for use, thus the Mongolian medicine has high use value and wide market prospect.
CN101029046A Substituted isoandrographolide derivative, its production and medicinal composition A substituted isoandrographolide derivative with high inhibition to cox-2 suppression, TNF-alpha and IL-6, its preparing process, and its medicinal composition are disclosed.
US7138376 Composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4'-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof A compound, method and composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4′-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
CN102633831A Methyl phosphorus propofol disodium dihydrate and preparation method and application thereof The invention provides a methyl phosphorus propofol disodium dihydrate and a preparation method and application thereof. The methyl phosphorus propofol disodium dihydrate can be crystallized in different modes to obtain multiple crystal forms, and can be used for preparing anaesthetic drugs.
CA2359363C 4-(heterocyclylsulfonamido)-5-methoxy-6-(2-methoxyphenoxy)-2-phenyl- or pyridylpyrimidines as endothelin receptor antagonists The compounds of formula (I) wherein R1, R2 and X have the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.
CN103006571A Poly(lactic-co-glycolic acid) encapsulated aspirin-temozolomide slow release microsphere and preparation method thereof The invention relates to a poly(lactic-co-glycolic acid) encapsulated aspirin-temozolomide slow release microsphere and a preparation method thereof. The preparation method comprises the following steps: weighing poly(lactic-co-glycolic acid), aspirin and temozolomide; dissolving in ethyl acetate to prepare a mixed solution; and performing spray drying through a spray dryer, thus finishing microsphere preparation, wherein the air inlet temperature is 43-45 DEG C, the air outlet temperature is 38-40 DEG C, and the microsphere preparation can be performed when the display of the air inlet temperature is the same with the display of a set temperature. The microsphere is uniform in size and smooth in surface, the particle size is 2.36+/-0.65 mu m, the medicament carrying rate is 26+/-0.45%, the encapsulation rate is 86.69+/-1.51, the microsphere has low toxic and side effect and favorable slow release effect, and the sustained release time is 500 hours. When being used with a certain dose of aspirin, the treatment effect of temozolomide can be enhanced, thereby avoiding the possible temozolomide dose-limiting toxicity. Thus, the invention provides a means for chemotherapy of glioblastomas.
WO2005089740A1 Coenzyme q composition with long-term persistence in blood To further ensure the achievement of the effects of coenzyme Q which is expected as highly contributing to human and animal health maintenance, it is intended to provide a composition capable of achieving a high concentration in the blood and a long-term persistence in the blood. Namely, a composition comprising coenzyme Q as a mixture of reduced coenzyme Q with oxidized coenzyme Q wherein the ratio of the reduced coenzyme Q exceeds 95% by weight to the total coenzyme Q. By using this composition, a high maximum coenzyme Q concentration in the blood can be obtained and, moreover, the concentration in the blood can be maintained at a high level and the area under the blood concentration curve (AUC) can be enlarged.
EP1368021B1 Carbamate compounds for use in preventing or treating bipolar disorder This invention is directed to a method for preventing or treating bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of an enantiomer of formula (I) or enantiomeric mixture wherein one enantiomer of formula (I) predominates wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).
EP0901474B1 Aryl pyrimidine derivatives The present invention is directed to pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, which exhibit useful pharmacological properties, in particular use as selective 5HT2B-antagonists, their preparation, pharmaceutical compositions comprising them and their use in the treatment of various diseases, especially migraine. The invention is also directed to formulations and methods for treatment.
WO2009014101A1 Novel sulfonated sugar derivative, and use thereof for medicinal agent Disclosed is a sulfoquinovosyl acyl propanediol derivative represented by the general formula (I) or a pharmaceutically acceptable salt thereof. (I) wherein R1 represents an acyl residue of a fatty acid; and M represents a hydrogen ion or a metal ion.
CN101982172A Combined drug of Ginkgolide and Ginkgo flavone as well as preparation and application thereof The invention discloses a combined drug of Ginkgolide and Ginkgo flavone as well as a preparation and an application thereof, relating to a composition method and a preparation method of a pharmaceutic preparation, particularly relating to a composition method of Ginkgolide and Ginkgo flavone as well as a preparation and an application thereof. The combined drug in the invention has the effective components of Ginkgolide (lactone extracts of Ginkgo leaves) and Ginkgo flavone (flavonoid extracts of Ginkgo leaves) in proportion, wherein the weight ratio of the Ginkgolide to the Ginkgo flavone is 3-1:2.3-10. The preparation is an oral preparation or an injection preparation and comprises medical auxiliary materials of oral preparation or injection preparation. The oral preparation comprises hard capsules, soft capsules, granules, pills, tablets, dispersible tablets and gastric floating tablets. The injection preparation comprises small volume injections, large volume injections and powder-needle injections. The invention also discloses the application of the combined drug of the Ginkgolide and the Ginkgo flavone in preparing drugs for curing blockage of collaterals caused by phlegm and blood stasis in coronary hear disease, angina pectoris and apoplexy.
EP1966179A2 Darifenacin hydrobromide composition substantially free of oxidized darifenacin and salts thereof and processes for the preparation thereof Provided are darifenacin hydrobromide free of oxidized darifenacin, and processes for the preparation thereof.
US6951853 DNA sequence selective agents as potential antitumor compounds Novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as well as processes for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids are dislcosed. More particularly, present invention relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as DNA sequence selective agents which are useful as potential antitumour agents. In particular, the present invention relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. These compounds have the formula XIV shown below:
EP1305301B1 Alpha-acyl and alpha-heteroatom-substituted benzene acetamide glucokinase activators Compounds fo the formula (I) wherein R?1 and R2¿ are independently hydrogen or substituents; R3 is lower alkyl having from 2 to 4 carbon atoms or a 5 to 7-membered ring which is cycloalkyl, cycloalkenyl, or heterocycloalkyl having one heteroatom selected from oxygen and sulfur; R4 is -C(O)NHR5, or is R6; R6 is a heteroaromatic ring connected by a ring carbon atom to the amide group and having nitrogen adjacent to the connecting ring carbon atom; and X is oxygen, sulfur, sulfonyl of carbonyl; are glucokinase acitvators useful for treating type II diabetes.
EP0914165B1 Steroids as neurochemical stimulators of the vno to alleviate symptoms of pms The invention relates to a method of alleviating the symptoms of PMS and anxiety. The method comprises nasally administering a steroid which is a human vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.
US20090036420 Benzamide derivatives and their use for treating cns disorders The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.
CN101584704B Medicinal application of medicinal salt or derivative of heparin and low molecular heparin The invention relates to an application of a medicinal salt or a derivative of heparin and low molecular heparin for preparing an oral medicament composition, belonging to the field of medicines. The oral medicament composition enables a diabetic to recover after long-time treatment of diabetes, can prevent a patient who has reduced sugar tolerance from becoming a diabetic and can improve the vitality of islet cell beta. The medicinal application of the medicinal salt or the derivative of the heparin and the low molecular heparin has significant treatment effect and is quite suitable for clinical application.
EP1015019B1 Compositions and methods of therapy for igf-i-responsive conditions Compositions and methods useful in therapy for IGF-I-responsive conditions in a mammal are provided. The method comprises concurrent therapy with both IGF-I or a variant thereof and at least one GAG to promote a desired therapeutic response with respect to a particular IGF-I- responsive condition. Concurrent therapy is achieved by admininstering to a mammal a single pharmaceutical composition containing both IGF-I (or a variant thereof) and at least one GAG according to a dosing regimen. Alternatively, IGF-I or a variant thereof and at least one GAG can be administered as two separate pharmaceutical compositions. A pharmaceutical composition comprising IGF-I or a variant thereof and at least one GAG for use in the IGF-I and GAG therapy is also provided.
WO2012162461A1 Phenyl-thiazolyl inhibitors of pro-matrix metalloproteinase activation This invention relates to phenyl thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis. Formula (I)
CN103520176A Application of compound in preparing lung cancer metastasis resistance medicine The invention discloses an application of compound in preparing lung cancer metastasis resistance medicine and belongs to the technical field of medicine novel applications. The compound is Asperterpenols A and can inhibit movement and metastasis of cancer cells. The application of the Asperterpenols A in preparing the lung cancer metastasis resistance medicine is disclosed for the first time and due to the fact that a framework type belongs to a totally novel framework type and the lung cancer cell metastasis inhibitory activity of the Asperterpenols A is high, the application has remarkable progress.
CN101756967A Application of methazolamide to preparation of medicaments for preventing and treating acute altitude diseases The invention relates to novel use of methazolamide, namely the application of the methazolamide to the preparation of medicaments for preventing and treating acute altitude diseases. The methazolamide can effectively reduce the symptoms of altitude stress, reduce the HR of crowds quickly entering plateau, improve SatO2 of the crowds, and decrease the occurrence of the acute altitude diseases, and the methazolamide has wide application prospect in the preparation of the medicines for preventing and treating the acute altitude diseases.
CN1872847A Compound of saturated bicyclic ring in cyclohexanone class, preparation method and application This invention relates to a method for preparing saturated dicyclic (endocyclic) cyclohexanol compounds, whose general chemical formula is shown in formula 1. The compounds can be used as cell cycle inhibitors, cell apoptosis inducers, cell proliferation inhibitors and antitumor drugs for antitumor therapy.
CN102949359A Cefditoren pivoxil tablet and its preparation method The invention relates to a cefditoren pivoxil tablet. The tablet comprises a tablet core and a coating layer, wherein the tablet core contains amorphous cefditoren pivoxil, a filler, a disintegrating agent, a solubilizer and a lubricant, and the filler is a mixture of D-mannitol and beta-cyclodextrin and/or low-substituted hydroxy propyl cellulose. The cefditoren pivoxil tablet avoids the conversion of amorphous cefditoren pivoxil to crystals and has good disintegration and dissolve-out properties under four dissolve-out conditions, and the dissolve-out curve of the cefditoren pivoxil tablet is consistent with the dissolve-out curve of a listed product Meiact.
CN102038679A Metronidazole, clotrimazole and chlorhexidine acetate vagina gel and preparation method thereof The invention discloses a metronidazole, clotrimazole and chlorhexidine acetate vagina gel and a preparation method thereof. Every 1000g of gel comprises the following components by weight: 40g of metronidazole, 32g of clotrimazole, 1.6g of chlorhexidine acetate, 10g of Carbomer 934, 120g of glycerol, 4g of triethanolamine, 1g of ethylparaben and the balance pure water. The method comprises the following steps: (1) mixing the metronidazole, clotrimazole and chlorhexidine acetate based on respective weight, and crushing evenly and sieving for later use; (2) preparing the Carbomer 934, triethanolamine and pure water into a matrix based on respective weight; (3) adding glycerol, ethylparaben into the crushed components in the step (1), and stirring evenly to obtain a mixture for later use; (4) adding pure water into the mixture of the step (3), mixing evenly to prepare into 1000g of gel; and (5) carrying out encapsulation on the gel obtained in the step (4) to obtain the product of the metronidazole, clotrimazole and chlorhexidine acetate vagina gel. The metronidazole, clotrimazole and chlorhexidine acetate vagina gel disclosed by the invention has excellent treating effects, and is a medicine which is convenient to use, is non-irritant, and has no foreign body sensation and good curative effect.
US6967248 Crystalline forms of meloxicam and processes for their preparation and interconversion The invention relates to the new crystalline forms II, III and V of meloxicam; to the processes for obtaining the crystalline forms I, II, III and V; and, finally, to the interconversion processes of the forms II, III, IV and V into the form I.
US7390808 Inhibitors of GSK-3 and crystal structures of GSK-3β protein and protein complexes The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
CN101249078A Sodium rebeprazole freeze-dried injection The invention relates to rabeprazole sodium lyophilized powder for injection, which is used to treat gastric ulcer, duodenal ulcer, stomal ulcer, reflux esophagitis and Zollinger-Ellison syndrome. The freeze-dried powder for injection contains rabeprazole sodium and meglumine in the mass ratio of 1:0.1-1. The preparation method of the freeze-dried powder for injection comprises the following steps of putting the meglumine in an aseptic container, adding water for injection for dissolution and homogenization, adding the rabeprazole sodium and other adjuvant materials, stirring for dissolution and homogenization, measuring intermediate content, filtering with a microporous membrane with a particle size of 0.22 mum under aseptic conditions if the intermediate content is qualified until filtrate is clarified, filling the filtrate in aseptic vials, sealing the vials partially with butyl rubber stoppers, loading on a disk, freeze-drying, boxing, sealing, testing quality and packaging.
CN101381348A Thiazolidone derivates and application thereof in preparing anti-lung cancer medicine The invention discloses a thiazolidone compound the chemical structure of which is shown by a general formula (I). The compound can selectively kill lung cancer cells and drug-resistant lung cancer cells which are over-expressed by P-glycoprotein, and have no obvious toxity on normal fibroblasts. The compound is a novel compound for starting an apoptotic signal transfer mechanism of tumor cells, is a potential anti-lung cancer medicine for selectively inducing apoptosis of the lung cancer cells and effectively treating refractory lung cancer, and has wide market application prospect.
WO2014100438A1 Cycloalkenyl hydroxamic acid derivatives and their use as histone deacetylase inhibitors The present invention provides compounds of formula (I) or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein W, X, n, s, t, and Ra are as described herein. The present invention relates generally to selective inhibitors of histone deacetylase and to methods of making and using them.
US7045631 Substituted 2-thio-3, 5-dicyano-4-phenyl-6-aminopyridines and their use as adenosine receptor-selective ligands Compounds of the formula (I) a process for preparing them, and their use as medicaments are described.
WO2014127360A1 Pcl compounds, compositions, and methods of use thereof Disclosed herein are compounds useful for detecting oxidants in a living cell, in a multicellular organism, or in a cell-free sample. In particular, disclosed herein are bioluminescent reporter compounds, and more particularly, fluorinated peroxy-caged- luciferin (PCL) compounds, compositions comprising such compounds, methods of using such compounds and compositions, and processes for preparing such compounds. Also disclosed herein are kits and methods for detecting and measuring peroxynitrite, and optionally, additional oxidants in a living cell, in a multicellular organism, or in a cell-free sample.
US7074391 Use of olive oil in the preparation of a product for oral hygiene for eliminating or reducing bacterial plaque and/or bacteria in the mouth The use of olive oil is described in the preparation of a product intended for oral hygiene, for example, a toothpaste, a mouthwash, a spray or oral inhaler or chewing gum, to eliminate or to reduce the bacterial plaque and/or bacteria present in the buccal cavity, achieving thereby a reduction in the occurrence of dental diseases (tooth decay, periodontal disease) and halitosis.
EP1712556A1 Azithromycin monohydrate Azithromycin in the form of a stable monohydrate and processes for the preparation of azithromycin in the form of an, e.g. stable, monohydrate.
WO2009084122A1 Iron-enriched composition It is intended to provide a composition for increasing the iron concentration in the blood including yeast containing iron in an amount of 0.3 g or more per 100 g of dry yeast. The composition of the invention shows better iron absorption compared with hem iron or water-insoluble inorganic iron which is equivalent in terms of amount of iron, and causes less stimulation to the stomach compared with iron sulfate (II) which is equivalent in terms of amount of iron. Therefore, it is suitable for the case of repeated administration, the case of administration on an empty stomach, or before during or after meals, and the case of administration to a subject for whom less stimulation to the stomach is desired.
EP2734519A1 Anti-biofilm compounds The present invention provides non-peptide compounds of formula (I) wherein: X is -(C1-C8)allcyl-, aryl or -aryl(C1-C8)alkyl-; Y is -(C1-C8)alkyl- or absent; W is heteroaryl, (C3-C7)carbocycle or aryl, wherein any heteroaryl, (C3-C7)carbocycle or, aryl of W is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) Z1 groups; R1 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, -CN, NO2, halogen, -ORa, -SRa, -S(O)2NRbRc, -NRbRc, -NRaCORd, -C(O)Ra, -C(O)ORa, and -C(O)NRbRc; R2 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)Jalkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, -CN, NO2, halogen, -ORe, -SRe, -S(O)2NRfRg, -NRfRg -NReCORh, -C(O)Re, -C(O)ORe and -C(O)NRfRg; I that mimic the streptococcal; SspB Adherence Region (BAR) and function as inhibitors of P. gingivalis adherence to streptococci. The invention also provides methods of making and using the inhibitors.
CN103705534A Preparation of natural active substance constructed polymer composite medicine and application thereof in inhibiting angiogenesis The invention discloses a preparation method of a natural active substance constructed polymer composite medicine and application thereof in inhibiting angiogenesis. The polymer composite medicine is formed by introducing natural active small molecule substances on carboxyl of heparin or derivatives thereof by a chemical coupling method. According to the polymer composite medicine, the dissolubility of the natural active small molecule substances can be improved, the toxic and side effects are reduced, the problem of bleeding after the heparin or derivatives thereof are massively used can be improved, and the effect of inhibiting angiogenesis when the heparin or derivatives thereof are used independently can be reinforced. The polymer composite medicine is simple in preparation process, easy to operate, can reduce cost and improve efficiency, and can easily realize industrialization.
CN102895476A Preparation method of medication alum and lotus root powder for treatment of rhinopathy The present invention relates to a preparation method of a medication alum and lotus root powder for treatment of rhinopathy. The method comprises: baking lotus root, leek seed and the like to brown; drying asarum, rice paper plant pith, and grinding with burntalum into extremely fine powder; and blowing the powder into nostrils. The medication has very significant effect on the treatment of rhinopathies such as nasal polyps and nasosinuitis.
CN102018671A Estradiol transdermal spray and preparation method thereof The invention discloses an estradiol transdermal spray, composed of the following raw materials in percentage by weight: 0.1-10% of estradiol, 0.5-10% of polymer, 0-20% of penetration enhancer, 0-10% of plasticizer and balance of solvent. The estradiol transdermal spray provided by the invention is applied to skin in a spray from, a uniform polymer thin film is formed after the solvent is volatilized, and medicine is dispersed in the film in a molecule form, so that not only the medicine transdermal penetration effect is improved and the blood concentration is sustained and stable, but also the patient compliance is good. The estradiol transdermal spray is filled in a spraying device and can be directly used, thus being easy and simple to use, and the dosage can be freely adjusted as required. The invention also discloses a preparation method of the estradiol transdermal spray, which has strong operability and low technological conditional requirements, and is simple and easy to realize and easy for industrialized production.
WO2014118578A1 Composition comprising a tnfr agonist and at least one thioredoxin inhibitor for use in the treatment of carcinoma. A composition for the treatment of cancerous cells, said composition including a combination of at least one Tumor Necrosis Factor receptor (TNFR) agonist and at least one thioredoxin inhibitor. This combinatorial approach involves direct inhibition of the Thioredoxin molecule (and not the enzyme of Trx reductase).
CN103263408A Allicin nano liposome and preparation method and application thereof The invention belongs to the technical field of liposome preparation, and discloses an allicin nano liposome and a preparation method and application thereof. The preparation method comprises the following steps of: (1) preparing a wall material solution, namely dissolving a wall material into chloroform, evaporating the wall material dissolved in the chloroform until a thin film is formed, then adding diethyl ether into the thin film, and redissolving the thin film to obtain the wall material solution; (2) preparing a core material solution, namely dissolving allicin into a mixed solution of absolute alcohol and a phosphate buffering solution to obtain the core material solution; and (3) preparing the allicin nano liposome by a reversed evaporation method, namely mixing the wall material solution prepared in the step (1) and the core material solution prepared in the step (2), performing ultrasonic treatment on the mixture until the mixed solution is clarified, rotatably evaporating the mixed solution to remove a solvent, adding a phosphate buffering solution (PBS) into the mixed solution, standing and filtering the mixed solution, and performing freeze-drying on a filtrate to obtain the allicin nano liposome. The allicin nano liposome prepared by the method has the advantages and beneficial effects of high wrapping rate, high stability, long-time storage, uniform and slow release process and the like and can be applied to the field of food, health protection products and medicines.
CN1990484A Silybin esters derivatives and preparation and use thereof The invention relates to a silibinin monoester derivative and its medicine salt or solvates. The invention also relates to its preparation method and its drug combination and medical application. The compound can inhibit activity of hepatitis b virus, so it is expected to be used as drug to treat hepatitis b virus and relevant virus diseases. The compound can protect liver and is expected to be used as drug preventing liver damage. The compound possesses effect anti free radical and is expected to be used as drug treating diseases caused by free radical.
US6949562 Heterocyclic compounds as ligands of the GABAA receptor Disclosed are heterocyclic compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, T, G, Q, W, Z, b, n and m are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptor.
US7189711 Muscle relaxants; central nervous system disorders; Parkinson's disease; Alzheimer's disease; strokes The invention refers to novel 2,3-benzodiazepine derivatives of formula (I) and pharmaceutical compositions containing the same as the active ingredient. The novel compounds antipasmodic, muscle relaxant and neuroprotective activities. In formula I; X represents a hydrogen atom, a chloro atom or a methoxy group; Y stands for a hydrogen atom or a halo atom; Z means a methyl group or a chloro atom; R is a C1-4 alkyl group or a group of the formula —NR1R2, wherein R1 and R2 represent, independently, a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group or a C3-6 cycloalkyl group.
CN1785188A Compounding metformin glipidide prepn. for treating diabetes type II, and its prepn. method A compound medicine for treating diabetes B is prepared from flumamine hydrochloride, glipizide, the extract of cinnamon bark and auxiliary. Its preparing process is also disclosed.
US20090306188 Importation of mitochondrial protein by an enhanced allotopic approach The inventors demonstrate that mRNA sorting to the mitochondrial surface is an efficient way to proceed to such an allotopic expression, and that this mRNA sorting can be controlled by selecting appropriate mitochondrion-targeting sequence (MTS) and appropriate 3′UTR sequences. The CDS sequence which codes for the protein to be delivered into the mitochondrion is guided by these appropriate MTS and 3′UTR sequences from the nuclear compartment to the mitochondrion-bound polysomes (where the CDS is translated), and aids in an efficient translocation of a mature functional protein into the mitochondria. Appropriate MTS and 3′UTR sequences correspond to those of nuclearly-transcribed mitochondrially-targeted mRNAs. The inventors demonstrate that, to obtain a stable therapeutically-effective importation, both an appropriate MTS and an appropriate 3′UTR should preferably be used.
US20070244103 Novel Compounds Having an Anti-Bacterial Activity The present invention describes novel anti-bacterial compounds of formula (I). Q-A-R3 (I) These compounds are, amongst others, of interest as inhibitors of DNA gyrase.
WO2012097331A1 Methods for increasing reticulocyte hemoglobin content The invention relates to methods and compounds useful for treating deficiencies in hemoglobin production. Methods and compounds useful for increasing reticulocyte hemoglobin content are provided.
WO2009089537A2 Anti-cancer compounds The present invention relates to anti-cancer compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides analogs of the known anti-cancer compound amonafide, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with hyperproliferation.
US20120208773 Pharmaceutical compositions with tetrabenazine The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.
CN103169683A Sodium ilaprazole enteric orally disintegrating tablet and preparation method thereof The invention relates to a sodium ilaprazole enteric orally disintegrating tablet and a preparation method thereof. The sodium ilaprazole enteric orally disintegrating tablet comprises the components in percentage by weight as follows: 1-5% of sodium ilaprazole, 8-10% of hollow pill core, 2-5% of stabilizer, 10-15% of isolating layer, 15-20% of enteric coating, 35-70% of filler and 10-20% of disintegrating agent. The invention provides the sodium ilaprazole enteric orally disintegrating tablet which is small in grain size, quick to absorb, high in bioavailability, good in taste, easy to swallow, good in disintegrating effect, strong in compressibility and convenient for patients to take, and the preparation method thereof.
WO2013134047A3 Aminoquinoline derivatives and uses thereof Described herein are aminoquinoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegerative diseases or disorderes, inflammation, inflammation associated diseases and disorders, and/or diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome.
US20120184518 Methods of treating or preventing an inflammatory disease or condition using glutaminyl cyclase inhibitors Methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.
CN101538303A Natural fatty acid monoester derivatives of cucurbitacin monomers The invention belongs to the technical field of medicaments and provides novel cucurbitacin B, E, Q and I natural fatty acid monoester derivatives of cucurbitacin monomers, which are prepared by bonding saturated or non-saturated natural fatty acid substances to cucurbitacin monomer structures through ester bonds formed in an acylation reaction or esterification reaction. The anti-cancer pharmaceutical composition of the invention contains a therapeutically effective amount of the derivatives of the cucurbitacin monomers and pharmaceutically acceptable carriers thereof. As the natural fatty acid substances can be actively taken up by tumor cells as in-vivo energy substances, the derivatives, bonded with natural fatty structures, of the cucurbitacin monomers (cucurbitacins B, E, Q and I) can be taken up by the tumor cells; and ester bonds break under the action of in-vivo esterase to release drugs; thus, the targeting of the drugs is realized so as to concentrate the drugs in the tumor cells and to greatly reduce the distribution of the tumor cells in normal tissues. Compared with the cucurbitacin monomers including cucurbitacins B, E, Q and I, the derivates has increased therapeutic indexes and greatly reduced toxicity.
CN102416090A External ointment for treating burn The invention relates to external ointment for treating burn and the technical field of external ointment. A preparation process comprises the following steps of: mixing the following medicinal materials in percentage by weight: 2 percent of glossy ganoderma, 2 percent of Sinkiang arnebia root, 3 percent of medcinal evodia fruit, 4 percent of ephedra herb, 1 percent of ginkgo seed and millet alcohol in a formula, soaking twice, mixing the two-time soaking solution, and mixing uniformly; adding medicinal material residues into water, and decocting twice; mixing the two-time decoction, mixing uniformly, cooling, adding 95 percent alcohol, mixing uniformly, standing, and filtering water extraction and alcohol precipitation liquid; mixing supernate and the soaking solution uniformly, heating liquid medicine, concentrating to prepare paste, adding 5 percent of deep sea mineral salt, 3 percent of pine oil, 5 percent of barbados aloe gel, 2 percent of ginseng extract, 3 percent of tung oil and 3 percent of swordlike atractylodes rhizome oil, and mixing uniformly; and decolorating by using active carbon until the mixture is colorless, adding 1 percent of borneol, 2 percent of menthol crystal and proper amount of rice vinegar, mixing uniformly, canning and sealing. The invention has the characteristics that the external ointment is health-care and convenient to use, and is used for sterilizing, diminishing inflammation, relieving pain and promoting blood circulation and removing obstruction in channels, and the precipitation of pigments on skin is avoided.
CN101204371B Vitamin C injection and preparation method thereof The invention discloses a vitamin C sodium squirt cut for injection and a preparation method, and the invention belongs to the field of the medical industry, and the invention relates to a vitamin squirt cut for injection and a preparation method, in particular discloses a vitamin C sodium squirt cut. The vitamin C sodium squirt cut comprises the vitamin C sodium, the anti-oxidant, the anti-oxygensynergistic agent and the water for the injection. The preparation method comprises three procedures which are the preparing of liquid medicine, the removing of the origin of heat and the split charging. Compared with the listed vitamin C sodium preparations, the vitamin C sodium squirt cut has the advantages of low cost and good stability, and the invention can be widely applied in the field ofthe medical industry.
US20100215746 Prevention of cisplatin induced deafness The present invention relates to compositions and methods for the protection and restoration of hearing. In particular, the present invention relates to methods and compositions for the prevention of chemical (e.g., cisplatin) induced deafness. The present invention thus provides methods of improving the outcome of subjects treated with cisplatin.
CN101392001A Carboxamides derivates, preparation method thereof and use on medicine The invention relates to a carbamylation derivative shown in general formula (I), a preparation method thereof, a medicine composite which contains the derivative and the applications thereof for being taken as a therapeutic agent particularly as a 5-HT4 receptor stimulant, wherein, each substituent in the general formula (I) is identical with the definition in a specification.
US7244744 Useful in treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels; treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides substituted piperidines, and compositions containing these compounds. Also provided are methods using the compounds of the invention for the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.
CN1634044A Pharmaceutical composition containing amoxicillin trihydrate and clavulanate potassium The invention discloses a slow release medicament three-layer tablet which comprises Amoxicillin hydrate, clavulanate potassium and pharmaceutically acceptable excipient or carrier, the layer 1 is a rapid release layer comprising Amoxicillin hydrate and clavulanate potassium, the layer 2 is a rapid release layer comprising a portion of Amoxicillin hydrate, the layer 3 is a rapid release layer comprising rest portions of Amoxicillin hydrate, the slow release layer contains not only common medicinal adjuvant, but also slow release material of hydroxy propyl methyl cellulose E30.
WO2010026075A1 Pyridine derivatives as inhibitors of hiv-i reverse transcriptase The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to Formulae I and II wherein Q, R1, R2, and R3 are defined as described herein.
CN102429868A Liposome medicinal composition with tumor targeting, in-vivo tracing and treating functions and preparation method thereof The invention discloses a liposome medicinal composition with tumor targeting, in-vivo tracing and treating functions and a preparation method thereof. The medicinal composition is a liposome targeting medicament which is resistant to CD44 antibody coupling, has a molecular imaging function simultaneously, and can be used for monitoring the in-vivo distribution of a medicament in real time in a living body state. In particular, plasmids containing three fusion genes, including renilla luciferase, red fluorescent proteins and suicide gene thymidine kinase, are coupled to CD44 antibody mediation-resistant immunoliposome, the specificity of liposome nanoparticles in a liver cancer in-situ model of an in-vivo targeting NOD/SCID (Non-Obese Diabetic/Severe Combined Immune-Deficiency) mouse is monitored by detecting a renilla luciferase signal with a living body imaging system, and apoptosis of liver cancer cells is induced by applying target thymidine kinase of ganciclovir; and moreover, a targeted liposome can be coated with adriamycin for inducing apoptosis of the liver cancer cells. The liposome medicinal composition provided by the invention does not have any toxic or side effect, has small damage and a good effect, and is suitable to be applied for a long time.
US7179842 Method of treating non-insulin dependent diabetes mellitus with phytanic acid derivatives The present invention is a method for the treatment or prevention of preferably non-insulin dependent (NIDDM or so-called Type II) diabetes mellitus, or other conditions associated with impaired glucose tolerance such as obesity, and in particular to the use of phytanic acid derivatives for the said treatment and/or prevention. A method of making a composition for the treatment or prevention of non-insulin dependent diabetes mellitus and related diseases comprising combining phytanic acid or derivatives thereof with a pharmaceutically acceptable additive or adjuvant, and a composition for the treatment or prevention of non-insulin dependent diabetes mellitus comprising phytanic acid or derivatives thereof are also provided.
CN101863927A Palladium coordination compound for antitumor drugs The invention belongs to the field of pharmaceutical science, and relates to a palladium coordination compound for antitumor drugs. The structural formula of the palladium coordination compound is shown in the specification, wherein a substituent group N-N is independently selected from aliphatic diamine or substituted aliphatic diamine, aromatic diamine and various substituted aromatic diamine; and an R1 or R2 is independently selected from substituted or unsubstituted branched chains and linear chain or cyclic annular aliphatic hydrocarbon, aryl groups, and nonaromatic or aromatic heterocycle groups.
US6939567 Pharmaceutical ayurvedic preparation The present invention relates to a process on ayurvedic preparation comprising in the steps of subjecting silver, mercury, sulphur and arsenic trisulphide to the steps of detoxification, grinding the detoxified mercury and silver in the presence of a citrus juice and then adding detoxified sulphur and again subjecting to the step of grinding to obtain a greyish black powder, adding detoxified arsenic trisulphide thereto and subjecting to the step of grinding, imparting a shape such as a ball thereto, coating the ball with detoxified sulphur in the presence of a citrus juice and subjecting the coated ball to the step of slow firing, adding detoxified arsenic trisulphide and firing, repeating said step of addition and firing ground in a citrus juice such that the weight of the ball is reduced by at least 10% to obtain an intermediate, adding serpentive and delphenium root thereto.
US7572790 Biphenyl carboxylic amide p38 kinase inhibitors Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
CN100575350C Macrocyclic glyceride with oxidization resistant activity and its preparation method and use The present invention discloses macrocyclic glyceride, namely, 1,2-cycle-(4,7 -cis-diene-9-alcohol-) cetane-diacyloxy-3-(cis-9-en-) octadecyl-diacyloxy-glyceride. The preparation method of macrocyclic glyceride is that the petroleum ether extract of the euonymus plant dwarf seeds is isolated through column chromatography by using 200 to 300 mu column chromatography silica gel, and then petroleum ether/acetone elution with volume ratio of 10 to 16:1 is used to collect the ingredient of 0.3 - 0.5 Rf, then macrocyclic glyceride is gained after the purification by methanol. The macrocyclic glyceride can effectively remove free radicals and is provided with antioxygenation. The macrocyclic glyceride can be a potential antioxidative drug, which can possibly reduce DNA damage caused by hydroxyl free radical oxidation.
CA2258892C Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (als) Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (ALS) are disclosed.
EP2748156A1 Novel piperidino-dihydrothienopyrimidine sulfoxides and their use for treating copd and asthma The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is CI and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
CN103340977A Buccal tablet applicable to being taken for type II diabetes The invention discloses a buccal tablet applicable to being taken for type II diabetes. The buccal tablet is prepared from the following components in parts by weight: 18-22 parts of island stichopus japonicas sea cucumber fucoidan chitosan sulfate, 17-19 parts of astragalus polysaccharide, 14-16 parts of rehmannia extract, 15-16 parts of tremella polysaccharide, 9-12 parts of microcrystalline cellulose, 7-9 parts of newtol, 7-9 parts of magnesium stearate, 4-5 parts of sodium citrate, and 0.3-0.5 part of peppermint essence. By adopting the buccal tablet disclosed by the invention, the fasting blood-glucose content of the mice with the type II diabetes can be obviously reduced; the tolerance dose of oral glucose is improved; C peptide and fasting insulin level in the blood are increased. Therefore, the buccal tablet has the advantages of being convenient to take, easy to store, high in bioavailability, convenient to carry, and suitable for living demands of fast-paced people.
US7635491 Method for administering selenium for treating patients suffering from systemic inflammatory response syndrome (SIRS), and composition for implementing the treatment The invention concerns the use of at least a molecule containing selenium, in an amount corresponding to a daily dose of about 2 to 40 mg, even 80 mg of atomic selenium equivalent, on its own or combined with other synergetic molecules for controlling oxidative stress and excessive inflammatory reaction: zinc, vitamin E, vitamin C, iron binder, glutathione precursor, copper and/or copper input binder, for preparing a medicine for treating severe systemic inflammatory response syndrome, in particular any acute infectious condition endangering the patient's life whether of bacterial, parasitic, fungal or viral origin, and any condition corresponding to a severe onset of inflammatory pathology bringing about an exacerbation of cytokine secretion. The invention is applicable in human and veterinary medicine.
CN101822747A Sugar-free wind-eliminating and itching-relieving granule The invention discloses a sugar-free wind-eliminating and itching-relieving granule, belongs to the field of medicaments, overcomes the defects that the traditional wind-eliminating and itching-relieving granule contains large amount of sugar and is not suitable for itching patients accompanying diabetes mellitus, hyperlipidemia, obesity, decayed tooth and the like to take. In the invention, a sugar-free accessory is screened to replace sugar powder in the traditional standard and a non-sugar sweetener is selected to correct the taste. In addition, the invention has the characteristics of good taste, no sugar and safe use and enlarges the application range of the wind-eliminating and itching-relieving granule.
US20120094948 Analogous Compounds of 6-Thioguanosine Triphosphate, their use in Medical Fields and Processes for their Preparation The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III). And wherein X represents either carbon or nitrogen atom within aromatic ring, Y represents either oxygen or sulphur atom and an additional group Q, group Qi or groups Qi (Qi indicates that the group or several groups may be bound to any unsaturated moiety of the ring) are selected from the group consisting of —OH, —COOH, —N(CH3)2, —N(CH2—CH3)2|—CO—CH3, —CO—O—CH3, —O—CH3, —S—CH3, —SO2—CH3, —CN, —NO2 or -Halogen elements, and wherein R5 may be formula (IV) and metal and ammonium salts thereof, wherein n is between O and 5, or oxygen or phosphorus is partially or completely replaced by nitrogen, sulphur, methyleno groups or their derivatives. The invention also concerns the uses of the above mentioned compounds in medical field and the process for their preparation.
US7011839 Combination of an antimicrobial, especially a quinolone antibiotic, and silver sulfadiazine Disclosed herein is an improved composition that is useful in treating otic infections comprising an antimicrobial and silver sulfadiazine in a therapeutically effective combination to treat otic infections in animals, the improvement comprising the composition which can be used safely to treat animals with a ruptured tympanic membrane.
CA2474608C Topical compositions comprising a plant extract for skin irritation or improvement of skin appearance There are disclosed topical compositions for alleviation of skin irritation symptoms or conditions having at least one plant extract effective to inhibit COX-2 enzyme, NGF protein, and/or TNF-alpha protein activity. Preferably, the compositions have a cosmetically, dermatologically, or pharmaceutically acceptable vehicle. In addition to the enzyme inhibitory plant material and acceptable vehicle, compositions may also have at least one active ingredient known to produce skin irritation. There is also a method for treatment of skin irritation symptoms or conditions involving topically applying compositions of the invention. Also disclosed are compositions and methods for topical administration of compositions to the skin that improve the aesthetic appearance of skin and/or provide an antiaging benefit to the skin.
WO2013190068A1 Probiotic and polyphenol against neurodegeneration The present invention relates to a composition comprising the probiotic strain Lactobacillus johnsonii CNCM I-1225 in combination with a polyphenol for use in the treatment or prevention of a cognitive and/or neurodegenerative disorder, in particular Alzheimer's disease.
WO2008032817A1 Sugar chain having activity against helicobacter pylori It is intended to provide a novel sugar chain which has an activity against Helicobacter pylori and a method of producing the same. Namely, a compound represented by the following general formula (1) is provided: (1) wherein Ac represents an acetyl group.
CN102309491A Tegafur and gimeracil compound injecta The invention discloses tegafur and gimeracil compound injecta, comprising tegafur, gimeracil, one or several kinds of auxiliaries suitable for injecta, and the balance of water for injection, wherein the tegafur and the gimeracil serve as active constituents, and the tegafur and gimeracil compound injecta is characterized in that the molar ratio of tegafur to gimeracil to oteracil potassium is 1:(0.2-0.4):1.
CA2783701A1 Selective beta-glucuronidase inhibitors as a treatment for side effects of camptothecin antineoplastic agents Compounds, compositions and methods are provided that comprise selective ß-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ß-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ß-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.
WO2006040534A3 Method of detecting the presence or activity of g - protein coupled receptor 92 (gpr92) We describe a method comprising detecting GPR92 modulated expression of an NF-κB, API, CRE or p53 sensitive reporter, preferably for detecting the presence, quantity, activity or a change in any of these of a GPCR. These methods are useful for identifying agonists and antagonists or inverse agonist of GPCRs. We also provide cells for use in these methods.
US7019156 Complex derivatives of bis(2-acetylpyridinethiosemicarbazonato-N1,N2,S)gallium(III) as anticarcinogenic agents The invention relates to a compound of the general formula (I) where R1, R2, R3, R4, R1′, R2′, R3′ and R4′ are independently of one another hydrogen, C1–C15-alkyl, C2–C15-alkenyl, C2–C15-alkinyl, C3–C16-cycloalkyl, C3–C16-cycloalkenyl, aryl or a heterocyclus which in each case can be substituted or unsubstituted, Y is a physiologically compatible anion, and n is 1 or 2, as well as its application to the prophylaxis and/or tretment of cancer illnesses.
CN101224233A Cassia plant extract and extracting method thereof The invention relates to an extract of cassia plant and an extraction method thereof. The extract can be used for the treatment of obesity, consists of one or a plurality of anthraquinones and contains by weight percentage: i) at least 1 percent of Orange obtusin, ii) at least 0.05 percent of obtusifolin, iii) at least 10 percent of total anthraquinone. In addition, the invention also discloses a method for extracting active component from cassia plant. The extract of the invention is a natural weight reduction combination and has good weight reduction effect, and can be produced into drugs, food replenishers, functional foods or drinks, cosmetics, etc. in various formulations.
CN103385906A Drug for shortening sow labor process and preparation method thereof The invention discloses a drug for shortening a sow labor process and a preparation method thereof. The preparation method comprises the following steps of adding 88.8806-88.8810% of injection water into a concentration tank, carrying out stirring, slowly adding 0.1-0.3% of metronidazole into the concentration tank, carrying out heating boiling, adding 9-11% of weighed glucose, 0.008-0.012% of triphosadenine, 0.006-0.01% of dexamethasone and 0.8-1.0% of common salt into the boiling solution until complete dissolution, adding active carbon of which humidity is pre-adjusted into the mixed solution for decoloration, filtering the hot mixed solution by a concentration and filtration titanium rod, collecting the filtrate by a dilution tank, carrying out stirring by the dilution tank, diluting the filtrate by injection water until the diluent filtrate volume is 90% of the total dilution tank volume, adjusting a pH value to 6.0-7.0 by a sodium hydroxide solution having the content of 0.1mol/L, carrying out dilution until the diluent filtrate volume is equal to the total dilution tank volume, adding active carbon of which humidity is pre-adjusted into the diluent filtrate for decoloration, carrying out filtration by a filter membrane until the filtrate is clear and transparent, feeding the filtrate to a soft bag liquid-conveying production line by a delivery pump, and carrying out loading.
CN103720644A Betamethasone sodium phosphate injection The invention belongs to the technical field of drug preparations and in particular relates to a betamethasone sodium phosphate injection. Every 1,000 ml of the betamethasone sodium phosphate injection contains 4.734-5.786 g of betamethasone sodium phosphate, 0.2-0.3 g of sodium hydrogen sulfite, 250-350 g of propanediol, a proper amount of a sodium hydroxide solution and the balance of injection water. The betamethasone sodium phosphate injection is good in stability, and the content of an effective ingredient-betamethasone sodium phosphate in the injection is basically stable and is not remarkably reduced through long-term experimental observation; a preparation process is simple and easy to control, the requirement on equipment is low, and the production cost can be reduced.
CN101810860A Medicinal composition having tumor-resistant synergy The invention relates to a medicinal composition having tumor-resistant synergy. The composition consists of a lidamycin olefin diyne type antibiotic, a geldanamycin benzoquinone ansamycin type antibiotic and derivatives thereof. Research shows that the geldanamycin benzoquinone ansamycin type antibiotic and derivatives thereof, which serve as a chemical therapy sensitivity enhancer, can inhibit the restoration of the DNA damaged by DNA damage medicaments, and achieve a synergic effect for treating tumor when used in combination with the chemical therapy medicament of the lidamycin olefin diyne type antibiotic.
CN101289444B Pyrimidine derivate and medicinal use thereof The invention discloses a pyrimidine derivative as the formula (I), wherein, the formula (I) is shown, the pyrimidine derivative can be used for preparing medicines for treating related diseases of angiogenesis, particularly used for preparing medicines for treating tumors or the aging macular degeneration.
CN102872161A Sterilizing tissue containing herbal ingredients The invention relates to a sterilizing tissue containing herbal ingredients. A non-woven fabric is taken as a base material. The sterilizing tissue is characterized by comprising chlorine dioxide, 1 to 1.5 percent of mint leaf extracts, 2 to 4 percent of propylene glycol, 0.5 percent of trichloro hydroxyl phenylate, 1 to 2 percent of borneol, 0.2 to 0.4 percent of Chinese mugwort leaf and 0.3 to 0.5 percent of Chinese gall. The sterilizing tissue also comprises a surfactant which is lauric acid fatty acid and/or glyceride. The PH value of the sterilizing tissue is 6. Active ingredients such as chlorine dioxide and trichloro hydroxyl phenylate are added into the sterilizing tissue containing herbal ingredients, and are spectral bactericides which are high in efficiency, low in toxicity and quick in sterilization, and the sterilizing tissue is strong in sterilizing ability and pollution-free; the ingredients such as mint leaf extracts, borneol, Chinese mugwort leaf and Chinese gall are added into the sterilizing tissue, so that an effect of protecting skin is achieved, and the sterilizing tissue has continuous efficacy and a pleasant fresh scent.
CN103145732A Antifungal derivatives of piperazine, as well as preparation method and application thereof The invention belongs to the technical field of antifungal medicines, and provides piperazine derivatives with structures as shown in a formula I, and pharmaceutically acceptable salts of the piperazine derivatives. The definition of the R1 is in line with the description of the specifications. The invention also relates to a preparation method of the compounds, and also discloses pharmaceutical compositions which adopt the compounds or the pharmaceutically acceptable salts as the effective and active components, and application of the compounds or the pharmaceutically acceptable salts in service of antifungal medicines.
WO2006114402A1 Substituted octahydroisoindoles as antagonists of melanin concentrating hormone receptor 1 (mch1r) The invention relates to compounds of the general formula (I) wherein R1, R2, R3, Ar, and X are as defined herein, or a pharmaceutically acceptable salt, hydrates, geometrical isomers, racemates, tautomers, optical isomers, N-oxides and prodrug forms thereof. The compounds may be used for the treatment or prophylaxis of disorders related to the MCH1R receptor and for modulation of appetite. The invention also relates to such use as well as to pharmaceutical formulations comprising a compound of formula (I).
CN103169967A Composition for improving female rate of chick embryos and preparation of composition The invention relates to the field of biological preparations and in particular relates to a composition for improving a female rate of chick embryos and a preparation of the composition. The composition comprises benzoic acid estradiol, vitamin E, androgen receptor antibody and diaminocaproic acid. The composition provided by the invention can be used for remarkably improving the female rate of the chick embryos as well as enabling the female chicken of the converted chick embryos to continuously keep the female characteristics, so that the sexually-matured chicken can keep normal egg laying performance.
WO2007048779A1 Piperidin-4-yl-pyridazin-3-ylamine derivatives as fast dissociating dopamine 2 receptor antagonists The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
US20090030021 Quinazoline Derivatives and Therapeutic Use Thereof Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperproliferative disorders are also disclosed.
WO2013153111A1 Pharmaceutical composition containing an unsaturated fatty acid enriched with oxygen and an organic solvent The invention relates to a pharmaceutical composition containing an unsaturated fatty acid or a derivative thereof, wherein the unsaturated fatty acid is enriched with oxygen, and to an organic solvent. The oxygen enrichment is performed by means of treatment with ozone. The solvent is dimethyl sulfoxide (DMSO). The unsaturated fatty acid is preferably oleic acid. The invention further relates to products containing such a pharmaceutical composition and the use of the pharmaceutical composition, for example as a medical preparation. The pharmaceutical composition has antimicrobial (for example, antibacterial) properties.
CN1965856A Heparin sodium injection liquid used for venous retention needle The invention relates to a liquemin injection used in vein needle, wherein it can avoid pollution and obtain accuracy measurement. The invention is characterized in that: a, one ml injection contains 5-200 units of liquemin, while the pH range is 3-9; b, one bottle contains at least 4ml.
US20090117079 Methods and materials for treating or preventing diseases/disorders mediated by alcohol dehydrogenase The present disclosure relates generally to methods and materials for treating and/or preventing a disease or disorder in a subject that is mediated by alcohol dehydrogenase by administering to the subject a therapeutically effective amount of one or more agents that prevents and/or inhibits the metabolism of methanol by alcohol dehydrogenase. Methanol metabolism may be reduced/inhibited in a subject by administering to the subject a therapeutically effective amount of ethanol.
CN103191087A Application of aspidin PB in dryopteris fragrans in preparing antitumor medicines The invention relates to an application of aspidin PB in dryopteris fragrans in preparing antitumor medicines. According to the invention, through in-vitro activity screening and in-vivo tumor inhibition experiments, it is proved that aspidin PB has good activity against various tumor cells and especially MCF-7 human breast cancer cells. When aspidin PB is added into different excipients, the mixtures can be processed into any pharmaceutically acceptable preparation. Aspidin PB in dryopteris fragrans is safe and reliable, and has the characteristics of low toxic and side effect, clear treatment effect, wide antitumor spectrum, good resistance against various medicine resistances, and the like. Dryopteris fragrans has the advantages of rich resource, convenient collection, simple extraction process, and important industrialized development value.
US20120130147 Methods for the treatment of tumors with indane compounds Compounds of the formula (I), in which R1, R2, R3, R4, and q have the meanings indicated in Claim 1, can be employed, inter alia, for the treatment of tumours.
US8703119 Injectable biodegradable polymer compositions for soft tissue repair and augmentation Methods for soft tissue repair and/or augmentation using injectable, biodegradable polymers are described herein. In one embodiment, the polymer compositions are liquid or pastes at room temperature. In a preferred embodiment, the polymer composition contains liquid or pasty hydroxy fatty acid-based copolyesters, polyester-anhydrides, or combinations thereof. The viscosity of the polymers increases upon contact with bodily fluid to form a solid or semisolid implant suitable for soft tissue repair and/or augmentation. In another embodiment, the polymer composition contains particles of a polymer stereocomplex. One or more active agents may be incorporated into the polymer compositions. Suitable classes of active agents include local anesthetics, anti-inflammatory agents, antibiotics, analgesics, growth factors and agents that induce and/or enhance growth of tissue within the filled cavity or control the growth of a certain type of tissue, and combinations thereof. The polymer compositions may also contain one or more additives or excipients that modify the physical and/or mechanical properties of the polymer. The polymer compositions are typically administered by injection. The injectable polymers can be used for a variety of soft tissue repair and augmentation procedures.
WO2014012593A1 Alkyl substituted 3-hydroxypyridines for the treatment of depression The present invention relates to the use of compounds of formula (I) wherein R1 is selected from the group consisting of C1-8alkyl; R2 is selected from the group consisting of C1-8alkyl; R3 is selected from the group consisting of H and C1-8alkyl; and R4 is selected from the group consisting of C1-8alkyl; or a pharmaceutically acceptable salt thereof for the treatment of depression, preferably anxious depression.
EP2464351A1 Isothiozoles for treating conditions of the eye Disclosed herein are isothiozoles for treating conditions of the eye.
US8618284 Methods of preparing polymorphic form A of bazedoxifene acetate The present invention relates to methods of preparing polymorphic Form A of bazedoxifene acetate and polymorphic Form A prepared by such methods.
WO2006066924A3 Azole derivatives with antimuscarinic activity The present invention relates to compounds of formula (I) wherein R1, R2, x, X, Y and B are as defined in the description for the treatment of muscarinic acetylcholine receptor mediated diseases, in particular M3 muscarinic receptor mediated diseases.
US20100298289 Heterobicyclic compounds as histamine h4-receptor antagonists The present invention concerns heterobicyclic compounds of formula (I) processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
WO2011105902A3 Antagonists of complement component 8-beta (c8-beta) and uses thereof Disclosed are antagonists designed to inhibit or block expression of a mammalian complement component 8-beta (C8-beta). The invention has a wide range of uses including use in the preparation of a medicament for the enhancement of nerve regeneration following acute or chronic nerve damage in a mammal.
CN103705441A Beclomethasone dipropionate emulsifiable paste The invention discloses beclomethasone dipropionate emulsifiable paste. The beclomethasone dipropionate emulsifiable paste comprises beclomethasone dipropionate adopted as the active component, an oil-phase component, a humectant, an emulsifier, an aseptic and water, and is characterized by also comprising edetate calcium disodium.
WO2010130943A1 5-membered heterocyclic compound cyclopenta[c]pyrrolylalkylcarbamate derivatives, preparation thereof, and therapeutic use thereof The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m and p have a value of 1; n and o have the same value which is 0 or 1; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl group or a trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The present invention can be used in therapeutics.
EP1041995B1 Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric compounds comprise the formula (I), wherein: B is H, OH, OSiR13, a residue of an amine-containing target moiety or a residue of a hydroxyl-containing moiety; L1 and L2 are bifunctional linking moieties; Y2 is O or S; R2 is selected from the group consisting of C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloakyls, C1-6 substituted alkyls, C3-8 substituted cyloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy, and C1-6 heteroalkoxy; R9, R10, R13 are independently one of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy, and C1-6 heteroalkoxy; Ar is a moiety which when included in formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or one; and R11 is a polymer residue. The first prodrug is generated when the polymeric portion of the double prodrug is cleaved and the parent molecule is generated rapidly thereafter in vivo, as a result of a trialkyl lock type lactonization-type reaction.
CN101204216B Coffee partner containing octacosanol and manufacture method thereof The invention relates to a coffee mate which contains octacosanol and a preparation method thereof, belogning to the beverage field. The coffee mate which contains octacosanol can adopt the microcapsule form, the sucrose and the Beta-cyclodextrin are the materials of the wall, the octacosanol and the palm oil and other components are the core materials. The invention is characterized in that the invention does not contain trans fatty acid; the added natural active ingredient which is the octacosanol has the physiological actions of anti-fatigue, building up body strength and reducing blood cholesterol, etc. By drinking the coffee mate, the physical fitness of the tired person can be recovered quickly, and the speed of getting rid of fatigue is quick; the body metabolism can be adjusted and the physique can be improved by drinking the coffee mate chronically. The invention caters to the consumption demands of health and nutrition of modern consumers, and the invention also corresponds with the development direction of the prior beverage industry, and the market prospect is very bright.
CN101979366A Diarylheptanoid compounds in curcuma zedoary and medicinal application thereof The invention belongs to the technical field of medicines and discloses new diarylheptanoid compounds extracted and separated from Guangxi curcuma zedoary and application thereof in the field of medicines. The chemical structure of the diarylheptanoid compounds is determined by spectrum technology such as a high resolution mass spectrum, one-dimensional and two-dimensional nuclear magnetic resonance spectrum and the like, and a chemical method. The diarylheptanoid compounds can be combined with a pharmaceutically acceptable carrier to prepare clinically acceptable medicines for anti-inflammatory treatment. Experiments for inhibiting lipopolysaccharide-induced rat macrophage from synthesizing nitric oxide (NO) in vitro prove that: the diarylheptanoid compounds have high activity of inhibiting the nitric oxide from being generated, and can be used as anti-inflammatory medicines for preventing and/or treating human and animals.
WO2011150320A2 Activators of innate immunity The present invention includes IFN activating agents that activate expression of IFN-B, activate NF-κΒ expression, activate an innate immune response, activate the expression of one or more cytokines, and/or induce the expression of interferon beta (TFN-β) through a RNase L and/or MDA5-dependent pathway. Such IFN activating agents include single stranded RNAs that encode for conserved region Π of the L protein of a negative stranded RNA virus, including, but not limited to, viruses of the family Paramyxoviridae. Also included are methods of making and using such IFN activating agents and vaccine compositions including such IFN activating agents.
EP2260051A1 Glucopyranoside derivatives Disclosed are novel compounds of formula (I) in which X has the meaning indicated in claim 1. Said compounds are suitable as antidiabetics.
CN101822688B Compound tylosin injection for animals and preparation method thereof The invention relates to compound tylosin injection for animals and a preparation method thereof. The injection consists of tylosin, doxycycline hydrochloride, trimethoprim, aminophylline, dexamethasone sodium phosphate, organic solvent and injection water. As a dedicated compound preparation for animals, the injection has special effect for treating respiratory tract infection caused by livestock and poultry sensitive bacteria and mycoplasmosis of pigs and poultry. The method has the advantages of convenient use, short course of treatment, low drug resistance and the like.
US7629327 Chlamydia 60 Kda CRMP antigens and vaccine uses The present invention provides vaccines and methods for immunizing a host, including humans, against disease caused by infection by a strain of Chlamydia, specifically C. pneumoniae. The vaccine and method employ a 60 kDa cysteine-rich membrane protein of a strain of Chlamydia pneumoniae. Modifications are possible within the scope of this invention.
CN102190622A Water-soluble derivatives of edaravone, preparation method and application thereof The invention discloses a series of amino carbonic ether derivatives of edaravone capable of reacting with acid salt to form water-soluble derivatives, and a preparation method thereof. The water-soluble derivatives are represented by the general formula (I), wherein R represents H, methyl, ethyl, propyl, isopropyl, butyl or benzyl, and HB represents the acid capable of reacting with organic groups containing nitrogen to form salt. The compound disclosed in the invention has favorable water-solubility and has the same cerebral protective effect in animals with edaravone.
US20070054899 Aromatase inhibitor compounds and uses thereof The invention concerns the use of a compound of formula (I) inhibitor of aromatase for the preparation of a pharmaceutical formulation intended for treatment of cancer or psoriasis. It equally relates to compounds of formula (I), notably for their use as active ingredients of a medication.
WO2006113204A3 Thymidine derivatives for treatmemt of kaposi's sarcoma A method for the prevention or treatment of Kaposi's sarcoma or Kaposi's sarcoma-associated herpes virus infection by administering an effective amount of a cyclopropanated carbocyclic 2'-deoxynucleoside to an individual in need thereof is provided.
US20120232133 Delivery of proteins using adeno-associated virus (aav) vectors Disclosed herein are compositions, systems and methods for delivery of proteins of interest using adeno-associated virus (AAV) vectors.
US20120283323 Treating Learning Deficits with Inhibitors of HMG CoA Reductase The disclosure provides methods of treating cognitive disorders by administering a HMG CoA reductase inhibitor. Cognitive deficits treatable with the inhibitor compound include those associated with Angelman Syndrome, Neurofibromatosis-1, certain forms of X-linked mental retardation, tuberous sclerosis, Down Syndrome, autism, and attention deficit/hyperactivity disorder.
US20080039411 Use Of Resistin Antisense Oligonucleotides And/Or Sirna Molecules In The Treatment Of Rheumatoid Arthritis The present invention relates to the use of oligonucleotides antisense to part of the resistin gene and siRNA blocking the action of resistin for the treatment of Rheumatoid Arthritis. The present invention also relates to the determination of the onset of rheumatoid arthritis.
CN103724243A 4-methoxybenzaldehyde L-cysteine schiff base and preparation method and application thereof The invention provides 4-methoxybenzaldehyde L-cysteine schiff base and a preparation method and application thereof, and relates to 4-methoxybenzaldehyde L-cysteine schiff base. The relative molecular weight of the 4-methoxybenzaldehyde L-cysteine schiff base is 239. The preparation method comprises the following steps of: adding 99.90% of L-cysteine to water to dissolve to obtain an L-cysteine aqueous solution; adding absolute ethanol to obtain an L-cysteine ethanol solution; adding 4-methoxybenzaldehyde and absolute ethanol; heating though oil bath; performing suction filtration; precipitating and flushing; and recrystallizing and purifying through a petroleum ether aqueous solution to obtain the white solid 4-methoxybenzaldehyde L-cysteine schiff base. The 4-methoxybenzaldehyde L-cysteine schiff base can effectively inhibit the activity of mushroom tyrosinase and human tyrosinase in a test tube, can effectively lower the expression quantity of tyrosinase in human melanoma A375 and A875 cells, and is nontoxic to human normal liver cells L02 and KM mice. The 4-methoxybenzaldehyde L-cysteine schiff base is applied to the preparation of a brightening agent for whitening cosmetics, as well as the preparation of a medicine for treating incontinentia pigmenti.
CN101822675B Application of aporphine alkaloid, oxoaporphine alkaloid and derivatives thereof in preparing antibacterial medicines The invention discloses application of aporphine alkaloid, oxoaporphine alkaloid and derivatives thereof in preparing antibacterial medicines. The invention provides a new medical usage and develops a new application field for the known aporphine alkaloid, the oxoaporphine alkaloid, the derivatives thereof and pharmaceutically acceptable salts thereof. The compounds, such as the aporphine alkaloid, the oxoaporphine alkaloid, the derivatives thereof and the pharmaceutically acceptable salts thereof, have remarkable antibacterial activity for staphylococcus aureus and methcillin-resistant staphylococcus aureus, and the invention provides a new compound for seeking for a new antibacterial medicine.
CA2368688C Novel inhibitors of formation of advanced glycation endproducts (age's) Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences.The compounds of the present invention are represented generally by the formula: (see above formula) The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.
US20090239939 Combinations for introducing nucleic acids into cells Combinations of a carrier and a complex consisting of a nucleic acid molecule and a copolymer are described, wherein the copolymer consists of an amphiphilic polymer, preferably polyethylene glycol, and a charged effector molecule, in particular a peptide or peptide derivative, as well as their use for the transfer of nucleic acid molecules into cells.
US20120058978 Method for the treatment of central nervous system cancers and compositions related thereto Use of compounds disclosed herein, typically progesterone or analog or derivative thereof, in the treatment of central nervous system cancers, specifically neuroblastoma and glioblastoma is provided. The treatment offers a reduced toxicity as compared to the currently available chemotherapeutic agents. The progesterone may be administered alone or in combination with, or in conjunction with other therapeutic agents.
CN101006997A Compound taxol and its derivative docetaxel fat emulsion and preparation method The invention relates to complex paclitaxel and its derivates docetaxel intralipid which includes the following ingredients: paclitaxel or docetaxel, vegetable oil, solubilizing agent, lecithin, glycerine, and water for injection at a ratio of 0.5-10:10-100:10-100:10-20:20-25:700-950. The preparing method includes the following steps: stirring with high speed homogenating machine or ultrasonic oscillating to get the protogala; preparing the complex paclitaxel intralipid with high pressure homogenizer. The preparation is intralipid in O/W type which packages paclitaxel or docetaxel into the compound oil phase. The compound oil phase has good solubility for paclitaxel or docetaxel which has prevented the phenomenon of precipitation after diluting the emulsion; the ingredients of compound oil has the function of coordinated antitumous effect; it can also release the injecting irritative response, haemolysis and hypersensitiveness; it has the function of targeting which has increased the drug action.
CN101757630A Method for controlling discolouring of gentamycin sulphate injection for livestock in storage The invention discloses a method for controlling discolouring of gentamycin sulphate injection for livestock in storage, including the following steps: (1) analytically pure concentrated sulphuric acid solution is used for regulating pH of gentamycin sulphate injection in product concentration regulating tank, so that pH of finished product gentamycin sulphate injection is 3.5-4.8; (2) the obtained gentamycin sulphate injection with pH of 3.5-4.8 is subject to conventional procedures of dilution blending, packaging, sterilizing and cooling, thus obtaining gentamycin sulphate injection finished product. The invention solves the problem that colour of gentamycin sulphate injection is changed from the original clear to tiny yellow in different degrees or yellow when in storage by simple and effective technology, the gentamycin sulphate injection is maintained in uniform clear state, product quality is improved, no complex apparatus is required to be used, process is terse, and cost is low, thus creating economic value for enterprise and suiting to be widely used.
CN103211936A Chinese and western medicine composite preparation The invention relates to a Chinese and western medicine composite preparation for treating internal hemorrhoids, beriberi and burns or tumble injuries, and concretely discloses a Chinese and western medicine composite preparation. The Chinese and western medicine composite preparation comprises 10-20g of Rhizoma Coptidis, 8-12g of unprepared rehmannia root, 25-35g of borneol, 8-12g of salt rust, 8-12g of dark plum, 8-12g of Arisaema Cum Bile, 90-110 tablets of compound sulfamethoxazole, and 600-800g of water, wherein the salt rust is white salt marsh obtained after salt boiling. The Chinese and western medicine composite preparation has very good curative effects on patients suffering from internal hemorrhoids, eczemas, combined hemorrhoids, nervous dermatitis, beriberi, tumble injuries, burns and tinea, and is convenient to use.
US20100074907 Methods for Promoting Myelination, Neuronal Survival and Oligodendrocyte Differentiation Via Administration of SP35 or TrkA Antagonists This invention relates to methods for promoting myelination, neuronal survival, and oligodendrocyte differentiation and treating demyelination and dysmyelination disease by the administration of a TrkA antagonist. The invention also relates to methods of inhibiting or decreasing Sp35 expression by the use of a TrkA antagonist. Additionally, the invention relates generally to methods for blocking Sp35 and TrkA interaction and inhibiting or decreasing TrkA phosphorylation by the administration of a Sp35 antagonist.
CA2752148A1 Pharmaceutical compositions comprising (3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl)methanol Disclosed herein is a pharmaceutical composition comprising (3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl)methanol and methods of using the composition to treat chronic pain.
CA2752070A1 Foamable benzoyl peroxide compositions for topical administration Described herein are benzoyl peroxide compositions useful in the treatment of acne and other skin conditions, which exhibit enhanced stability, even under accelerated conditions. The compositions also exhibit reduced color formation, reduced irritation, and enhanced moisturizing properties. They can be formulated into a topical aerosol foam with inert, non-flammable propellants, such as hydrofluoroalkanes, and may be used in cosmetics or pharmaceuticals. Additionally, methods of formulating these compositions are described.
EP1636212B1 Cycloalkylsulfanyl substituted benzo¬b|thiophenes as therapeutic agents The present invention provides benzo[b]thiophenes of Formula (I), wherein R1, R2, R3, and L have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (I).
EP1284738A4 (+) naloxone and epinephrine combination therapy A composition formulated for dose-wise delivery to a breathing passageway of a human, the composition comprising a carrier solution containing (+)naloxone and a pharmacologically effective amount of at least one adrenergic agonist, the (+)naloxone and agonist forming a mixture in the carrier. The at least one adrenergic agonist is selected from the group consisting of epinephrine, isoproterenol, abluterol, aminophyline, beclomethasone, dyphylline, flunisolide, isoetharine, metaproterenol, oxtriphylline terbutaline, theophylline, pseudoephedrine, phenylephrine, ephedrine and norepinephrine. That composition is delivered by an atomizer means such as a liquid sprayer or inhaler to treat nasal congestion and asthmatic attacks. Further provided by the invention is a cardiovascular and respiratory stimulating composition for administration to a patient in doses, the composition comprising a pharmacologically effective concentration of (+)naloxone in a carrier solution. If necessary, the composition may also contain a pharmacologically effective amount of at least one adrenergic agonist.
CN102961282A Composition with penetration enhancing effect as well as preparation method and application thereof The invention relates to a composition with a penetration enhancing effect, which is prepared from the following substances in parts by weight: 1-20 parts of blumea balsamifera and 1-10 parts of pogostemon cablin. The invention further relates to a preparation method of the composition. The preparation method of the composition is simple and feasible and is convenient for industrial production. The invention further relates to an application of the composition. The composition disclosed by the invention has a good penetration enhancing function and small irritation, has the effects of diminishing inflammation and relieving pain, and removing scars and promoting tissue regeneration, and can be widely applied to various drugs and cosmetics.
US20100183580 Treatment of pigs for reducing the feed conversion ratio or increasing the growth rate The invention relates to a method for the non-therapeutic treatment of pigs for the purpose of reducing the conversion ratio of the feed used to raise the pigs and/or for increasing the growth rate of the pigs. The treatment comprises orally administering at least one glycine compound to the pigs, which glycine compound corresponds to the following formula (I) or to a salt or an ester thereof: wherein R1 and R2 are independently an alkyl, an alkenyl or a hydroxyalkyl radical containing 1 to 18, preferably 1 to 6 carbon atoms or wherein R1 and R2 form jointly together with the N atom a heterocyclic 5- or 6-membered ring. The glycine compound is preferably N,N-dimethylglycine (DMG).
EP2334642A2 Simplified one-pot synthesis of [18f]sfb for radiolabeling A non-aqueous single pot synthesis of [18F]SFB is set forth. The [18F]SFB produced with this method is then used, for example, to label a peptide or an engineered antibody fragment (diabody) targeting human epidermal growth factor receptor 2 (HER2) as representative examples of labeled compounds for use as an injectable composition to locate abnormal tissue, specifically tumors within an animal or human using a PET scan.
CN103694299A Steroid androgen receptor inhibitors and preparation method and medical application thereof The invention relates to the field of medicinal chemistry, and particularly relates to a series of steroid androgen receptor inhibitors and a preparation method and medical application thereof, and particularly relates to an application as a medicine for preventing or treating the androgen receptor-related diseases such as cell proliferation depending on androgen, hirsutism, acne, androgenetic alopecia and the like.
EP1934388A1 Method of drug design The invention provides a method of identifying biologically active compounds comprising: (a) designing a first library of compounds of formula (1) to scan molecular diversity wherein each compound of the library has at least two pharmacophoric groups R1 to R5 as defined below and wherein compound of the library has same number of pharmacophoric groups; (b) assaying the first library of compounds in one or more biological assay(s); and (c) designing a second library wherein each compound of the second library contains one or more additional pharmacophoric group with respect to the first library; such that the/each component of the first and second library is a compound of formula (1).
CN101057944A Medicinal composite for treating bromhidrosis and its producing method The invention relates to a pharmaceutical composition for treating bromhidrosis and process for preparation, wherein the composition is prepared from the following constituents (by weight proportions): dragon's blood resin, monkey blood, spikenard, lead monoxide, calomel, camphor, cuttle-bone, dried alum and water by the ratio of 10:8-11:25-35:45-55:8-12:8-12:25-35:10-20:250-330.
CN103565831A Composition for treating fish-farming anoxia The invention discloses a composition for treating fish-farming anoxia. The composition is used for overcoming the shortcomings that in the existing artificial fish farming, the situations of water quality deterioration and anoxia happen often, lots of fish die, the fish farming benefit is reduced, a low-cost, simple, convenient and effective counter measure is unavailable, and the like. The composition comprises the following raw materials in parts by weight: 70 parts of raw gypsum, 30 parts of alum, 50 parts of loess and 10 parts of borneol. The finished product of the composition is obtained through smashing and uniformly mixing the raw materials; the finished product is scattered in the water surface where the fish are according to the amount of 10 kilograms of product per 5000 kilograms of fish. The composition for treating the fish-farming anoxia, disclosed by the invention, is capable of preventing lots of fish in ponds, reservoirs and the like dying from anoxia; the composition is good in effect and is capable of preventing above 95% of fish dying from anoxia; the composition is simple and convenient to use and the use cost is reduced by above 70%.
EP2029607A1 Novel 8,10-diaza-bicycloý4.3.1¨decane derivatives and their medical use This invention relates to novel 8,10-diaza-bicyclo[4.3.1]decane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
CN103467320A 2,5-disubstituted cyclopentanone derivatives and applications thereof The invention belongs to the field of medicine technology, and relates to 2,5-disubstituted cyclopentanone derivatives represented by the general formula I and applications thereof. The derivatives represented by the general formula I can be used as active ingredients used in preparation of drugs for treatment and/or prevention of various cancers, such as breast cancer, lung cancer, colon cancer, rectal cancer, gastric cancer, prostate cancer, bladder cancer, uterine cancer, pancreatic cancer, ovarian cancer and the like; and the active compounds can be used as only anticancer drugs, or can be combinedly used with one or more other antitumor drugs. Combined treatment is achieved by carrying out simultaneous, sequence or separated administration of treatment groups.
US20110251287 Hci polymorphs of 3-((2-(dimethylamino)methyl (cyclohex-1-yl))phenol A crystalline salt of 3-[2-(dimethylamino)methyl(cyclohex-1-yl)]phenol and hydrogen chloride, preferably in a 1:1 composition, including various crystalline forms of this salt, processes for preparing the various crystalline forms of this salt, pharmaceutical compositions containing the various crystalline forms of this salt, and the use of this salt as a pharmacologically active agent in a pharmaceutical composition to treat or inhibit pain or other disorders or disease states.
CN101879157A Application of kaempferol The invention discloses application of kaempferol in preparing drugs for curing hyperlipidemia diseases, especially hyperlipidemia diseases with reduced serum triglyceride and increased serum high-density protein. The applicant finds that the kaempferol has remarkable curative effect. The invention simultaneously provides drugs for curing the hyperlipidemia diseases.
CN1813697A Terbinafine hydrochloride vagina gel, and its preparing and quality control method The present invention discloses a terbinafine hydrochloride vagina gel, its preparation method and quality control method. It is made up by using terbinafine hydrochloride, gel matrix, solvent, osmosis adjuvant, metal chelant and pH regulating agent through a certain preparation process.
US20070049583 Benzoxazine and benzothiazine derivatives and their use in pharmaceutical agents Compounds of formula (I), their tautomeric and isomeric forms and salts, as well as the process for their production and their use in pharmaceutical compositions, are described.
WO2012150707A1 Low molecular weight compound which promotes induction of differentiation of stem cells into insulin-producing cells and method for inducing differentiation of stem cells into insulin-producing cells using low molecular weight compound A purpose of the present invention is to provide a low molecular weight compounds which especially promotes induction of the differentiation of ES cells into insulin-producing cells. Another purpose of the present invention is to provide: a method for inducing the differentiation of ES cells into insulin-producing cells using the compound; and an agent for promoting induction of the differentiation into insulin-producing cells. Another purpose of the present invention is to provide the thus-induced insulin-producing cells. Provided are: an agent for promoting induction of the differentiation of stem cells derived from a mammal into insulin-producing cells, which contains a compound that is selected from the group consisting of dopamine metabolism inhibitors, serotonin metabolism inhibitors, acetylchotine, acetylcholine degrading enzyme inhibitors and acetylcholine receptor activators; and a method for inducing differentiation using the agent for promoting induction of differentiation.
WO2005004860A3 Novel solid pharmaceutical composition comprising amisulpride The invention relates to a novel solid pharmaceutical composition for oral administration of the active ingredient amisulpride, characterized in that it comprises at least one encased amisulpride particle and at least one pharmaceutically acceptable excipient which is adapted for orodispersible administration of the composition. The novel composition can, more particularly, be provided in the form an orodispersible amisulpride tablet.
CA2229590C Pharmaceutical composition containing inhibitors of interferon- gamma The present invention provides compositions and methods for promoting the healing of wounds or fibrotic disorders with reduced scarring, comprising inhibitors and inhibiting IFN-.gamma., together with compositions and methods for promoting the healing of chronic wounds, comprising stimulating and stimulators of IFN-.gamma..
CN103435553A Piperazine structure-based aryl formamide Raf kinase inhibitor and preparation method as well as application thereof The invention relates to the field of pharmaceutical chemistry, in particular to a diaryl urea compound (A), wherein the definitions of R1-R13, Ar and X are shown in the specification. The invention also discloses a preparation method of the compounds of the general formula (A), medicinal compositions containing the compounds and medical application thereof, particularly application as the Raf kinase inhibitor.
US20080085861 Gas1 polypeptides There is disclosed a method of inhibiting the lethal effect of expressing an otherwise lethal protein in a cell, said method comprising: (a) providing a cell, tissue or organism having (i) a nucleotide sequence encoding a Gas1 protein, or a functional equivalent, derivative or bioprecursor thereof, which is capable of inducing apoptosis in said cell and (ii) a further nucleotide sequence encoding a protein which is otherwise lethal to said cell in itself or in response to a lethal stimulus in the presence of Gas1; (b) inhibiting function and/or expression of said Gas1 protein or functional equivalent, derivative or bioprecursor thereof; and (c) expressing said sequence encoding said otherwise lethal protein.
US20090028851 Novel Antibodies Directed to the Mammalian Eag1 Ion Channel Protein The present invention relates to a particularly advantageous antibody, antibody fragment or derivative thereof, which specifically binds to/interacts with at least one epitope of the extracellular or intracellular domain or the mammalian EAG1 ion channel and to nucleic acid molecules encoding the same and to vectors comprising said nucleic acid molecules. The invention additionally relates to methods for the preparation of said antibody, antibody fragments or derivatives thereof and to pharmaceutical compositions comprising the same. Furthermore, the use of said antibody, antibody fragment or derivative thereof and also diagnostic compositions comprising said components are disclosed in the specification. The invention also relates to a method of assessing for the presence of EAG1 expressing cells and for a method of blocking EAG1 function in said cells. The invention further relates to a method of treating diseases with the help or said antibody or antibody fragment or derivative thereof.
CN103356999A Novel marine organism washing-free disinfection solution and its application Belonging to the technical field of disinfection, the invention discloses a novel marine organism washing-free disinfection solution. In view of the disadvantages of existing disinfection technologies, especially preoperative disinfection technologies, the invention provides the novel marine organism washing-free disinfection solution, which comprises the following active ingredients by mass: 0.5%-2% of chitosan, 1-4% of chitosan oligosaccharide, 2%-8% of baicalin, 0.5%-2% of prebiotics, 0.5%-1.5% of polyhexamethylene guanidine, 2%-5% of lysozyme and 1.5%-5% of a Polygonum cuspidatum extract. The disinfection effect is good. The disinfection solution disclosed by the invention can be used for sanitation disinfection or the hand disinfection or skin disinfection in preoperative disinfection. With excellent sterilization effect and lasting effect, the novel marine organism washing-free disinfection solution has very good application prospects and economic benefits.
WO2008051805A3 Triazolo-pyridazine protein kinase modulators The present disclosure relates to triazolopyridazine protein kinase modulators of Formula (I), methods of using these compounds to treat diseases mediated by kinase activity.
US8758753 Ganglioside associated recombinant antibodies and the use thereof in the treatment of tumors The present invention is related to the obtaining of modified antibodies by means of DNA recombinant technology from the murine monoclonal antibody P3 (MAb P3), produced by the hybridoma cell line deposited under Budapest Treaty with accession number ECACC 94113026, and from its anti-idiotype murine monoclonal antibody 1E10(MAbai 1E10), produced by the hybridoma cell line with deposit number ECACC 97112901, with the objective of achieving monoclonal antibodies which preserve the biological function of specifically binding the antigen of the original antibodies, but being at the same time less immunogenic. The chimeric antibodies of the invention contain the variable domains of the murine immunoglobulin and the constant regions of the human immunoglobulin; and those humanized, besides containing the constant regions of the human immunoglobulins, are modified in the murine framework regions (FRs), in particular, in those zones that could be in a T cell antigenic site, so that several positions of the FRS are human as well. These antibodies can be used in the diagnosis and therapy of different types of tumors. The present invention is also related to the use of the antibodies for therapeutic and diagnostic purposes.
WO2006115136A1 Allergy-suppressive composition, allergy-suppressive food and allergy-suppressive agent It has been confirmed in tests in human that 1-kestose has an effect of increasing the production of an immunoglobulin A (IgA) antibody, an effect of inhibiting the production of an immunoglobulin E (IgE) antibody, an effect of activating the growth of an enteral bifidus bacterium and an effect of ameliorating atopic dermatitis in infants and young children. Based on this finding, there are provided an allergy-suppressive composition, an allergy-suppressive food and an allergy-suppressive agent comprising 1-kestose. Since 1-kestose has the effect of increasing the production of an IgA antibody, the effect of inhibiting the production of an IgE antibody and the effect of activating the growth of an enteral bifidus bacterium, the composition, food and agent comprise 1-kestose as the active ingredient and are effective for the prevention of the development of allergic diseases including atopic dermatitis in infants and young children and the treatment of an allergic condition.
WO2009087379A2 Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R1 and R2 is H, and the other is selected from C1-8-alkyl, C3-6-cycloalkyl and C1-8-alkyl-C5-10-aryl; R3 is selected from tert-butylmethyl, zso-propylmethyl, sec- butyl, tert-butyl, cyclopentyl, cyclohexyl and 1-methylcyclopentyl; R9 is selected from the following: wherein: R4 is selected from C1-8-alkyl and C3-8-cycloalkyl; G is selected from: ) CH, ) CMe and N; E is selected from: O, S, ) SO2, )NH, )NMe and N-oxide ()N->O); J and R are independently selected from: )CH, N and N-oxide ()N-^O); and R41 is selected from amino, methylamino, dimethylamino, isopropylamino, isopropyl(methyl)amino, cyclopropylamino, cyclopropyl(methyl)amino, cyclopentylamino, morpholino, piperidin-1-yl, piperidin-1-ylmethyl, morpholinomethyl, 4-methylpiperazin-l-yl, 4-(2-methoxyethyl)piperazin-l-yl, 1- moφholinoethyl, l-(dimethylamino)ethyl, l-(methylamino)ethyl, 4-fluoro-l- methylpyrrolidin-2-yl, 4,4-difluoropiperidin-l-yl, piperidin-4-yl, l-methylpiperidin-4- yl, pyridin-3-ylamino, pyridin-2-ylamino, l-methylpyrrolidin-3-yl, methyl, isopropyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of various diseases.
CA2294670C Composition suitable as food integrator and for the treatment of intestinal disorders and alterations of the bacterial flora The subject of the present invention is a composition suitable as food integrator and for the treatment of intestinal disorders and alterations of the bacterial flora, characterized in that it contains as active principle a combination of Bacillus coagulans and lysine. According to a preferred embodiment of the invention, the composition is made by first subjecting the Bacillus coagulans to a culture in the presence of lysine in the germinative phase, and then bringing it back to the state of spore. A further subject of the present invention is a method for the growth and development of cultures of Bacillus coagulans in the presence of lysine, as well as the use of these bacterial cultures thus produced and developed in the preparation of compositions suitable both as food integrators and as pharmaceutical compositions.
WO2012045729A1 Imidazo [1, 2 -a] pyridine and pyrazolo [1, 5 -a] pyridine derivatives as trpv1 antagonists A compound of formula of formula (I) wherein A represents a single bond, a CH2 group or a CH (Me) group; X1 represents a hydrogen atom, a fluorine atom or a methyl group; X2 represents a hydrogen atom, a fluorine atom, a methyl group or a CH2OH group; X3 represents a hydrogen atom, a fluorine atom or a CH2OH group, and at least two of X1, X2 and X3 are hydrogen; Y represents a C atom and Z represents a N atom or Y represents an N atom and Z represents a C atom. R1 represents a halogen atom, a C1-4 alkyl group, a trifluoromethyl group or a trifluoromethoxy group, and R2 and R3 are each independently selected from a hydrogen atom, a halogen atom, a C1-4 alkyl group, a trifluoromethyl group or a trifluoromethoxy group. or a pharmaceutically acceptable salt or solvate thereof. salt or solvate thereof.
US20080255065 In combination with one or more anti-cancer therapeutics inhibits neoplastic cell proliferation; siRNA molecule decreased gemcitabine chemoresistance of pancreatic adenocarcinoma cells in vivo, demonstrating a synergistic effect when administered in combination with gemcitabine Small interfering RNA (siRNA) molecules that target a mammalian ribonucleotide reductase gene, and which are capable of inhibiting the expression of their target gene are provided. The siRNA molecules of the invention are capable of attenuating neoplastic cell growth and/or proliferation in vitro and in vivo and, therefore, can be used to attenuate the growth and/or metastasis of various types of mammalian cancers.
CN102772364A Fat emulsion of Paricalcitol, its preparation and preparation methods thereof The invention relates to a fat emulsion of Paricalcitol. The fat emulsion comprises oil for injection, an emulsifier, a stabilizer, an isoosmotic adjusting agent, and a pH adjusting agent. Emulsion droplets have an average diameter of 50nm-1000nm. The fat emulsion can be prepared into injection emulsions, freeze-dried emulsions or capsules. Specifically, organic solvents cannot be employed as injections so as to reduce stimulation on blood vessels during injection and avoid injection package material impurity leaching caused by organic solvents, thus ensuring product quality and safety, and reducing the difficulty of product quality control.
US7326791 Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions Substituted carboxylic acid amides of general formula wherein A, B, and R1 to R5 are as defined herein, and the tautomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, such as antithrombotic activity and factor Xa-inhibiting activity.
WO2007008111A3 Method of loosing weight The invention belongs to medicine and more particularly to processes of treatment of fatness; it can be used in all cases of excessive weight, with any concomitant diseases, as well as to help loosing weight people who wish to lose a few additional kilos. The invention allows to increase the effectiveness of gradual slimming for a number of wished kilos, to suppress the feeling of hunger, to clean the body of toxins and waste or to keep a given weight, and it ensures a better accessibility and a lower cost of the treatment thanks to the use of food additives including silicon gel proportioned between 100 and 1000 g, before and/or after each meal or in place of each meal, with a duration of treatment from 2 to 96 weeks.
EP2111387B1 New method for preparing unsaturated fatty hydroxy-acids The invention relates to a method for preparing a compound of the following formula (I) in which a and b are integers equal to or higher than 0, and R1, R2 and R8 essentially represent H, said preparation method including a step of oxidising the alcohol function of the compound of the formula (II-b) in which a, b and R2 are such as defined above in the formula (I), and R6 and R7 essentially represent a hydrogen atom, wherein said step is followed by a step comprising the implementation of a Wittig-Horner reaction, a step comprising the oxidant cut of the double bond and a reduction step.
WO2008010768A1 Method of treating and diagnosing restless legs syndrome and periodic limb movements during sleep and means for carrying out the method A method of treating Restless Legs Syndrome and/or Periodic Limb Movements during Sleep (RLS) comprises administration of a therapeutically effective dose of biologically active zonisamide and a dopaminergic agent selected from dopamine agonist and dopamine turnover promoting agent including dopamine uptake inhibitor over an appropriate period of time, such as a period substantially coinciding with the period of sleep of said patient. Also disclosed is a corresponding method of treatment, the use of biologically active zonisamide and a dopaminergic agent selected from dopamine agonist and dopamine turnover promoting agent including dopamine uptake inhibitor for the manufacture of a medicament for treating RLS, and a corresponding method of manufacture.
WO2006111296A2 Dosage forms and combined preparations of pyrimidine biosynthesis inhibitors for achieving additional effects upon the immune system The invention relates to a pharmaceutical preparation containing at least one pyrimidine synthesis inhibitor such as leflunomide, whereby the pyrimidine synthesis inhibitor causes a rise in the blood plasma level from 1.1 mg/liter to 5 mg/liter within an hour after oral administration to humans.
CN101919802A Solid effervescent mixture for the oral absorption The invention relates to an effervescent mixture, specifically relates to a solid effervescent mixture for the oral absorption and preparation method thereof. The invention comprises the alkalic component of a mixture consisting one or more than one of alkali metal carbonate, alkali metal bicarbonate, alkaline earth metal carbonate or pearl powder; the acid component of a mixture consisting one or more than one of tartaric acid, citric acid, adipic acid, fumaric acid, maleic acid, malic acid, folic acid andacid phosphate; The medical component of a mixture consisting of one or more than one of vitamin C, glucurolactone, natural caffeine, haw extract, green tea extract, hovenia acerba extract, semen myristicae extract, Poria cocos extract, Amomum tsao-ko extract, root of kudzu vine extract, spina date seed extract, cassia twig extract, Lesser Galangal Rhizome extract, and chrysanthemum extract; the wrapper and auxiliary material of a mixture consisting one or more than one of polyethylene glycol (PEG), panthenol and glycerin monostearate. The invention comprises, by weight, 5-50% of alkalic component; 5-50% of acid component; 1-40% of medical component; 0.5-35% of wrapper; 1-10% of auxiliary material. The invention has advantages of being fast in effect, and convenient in medicine taking and carrying.
CN102670513A Ofloxacin molecular inclusion nanometer preparation and preparation method thereof The invention relates to an ofloxacin molecular inclusion nanometer preparation and a preparation method thereof, belonging to the technical field of medicines. The main raw materials of the molecular inclusion nanometer preparation are cyclodextrin, solubilizer, polymer materials, ofloxacin and the like. The preparation method comprises the steps of: adding the cyclodextrin after dissolving the ofloxacin in a solution containing the solubilizer and preparing a molecular inclusion compound through a gradient ultrasonic grinding method; then adding the polymer materials for grinding; and drying and smashing to obtain the ofloxacin molecular inclusion nanometer preparation. The average particle size of the molecular inclusion nanometer preparation is 252.3 nm; and the drug content is 1%-25%. The preparation method, disclosed by the invention, has the advantages of being simple in a preparation process, high in drug carrying amount and stability, controllable in quality, suitable for industrial production and the like. The ofloxacin molecular inclusion nanometer preparation prepared by the method has the advantages of efficiently improving stability of the drug and dissolution degree as well as dissolution speed of the drug in a gastrointestinal tract, improving a drug absorption rate, realizing rapid and efficient effects, masking bitter taste of the drug, reducing drug irradiation and improving drug palatability and drug availability.
CN103284960A Vincristine freeze-dried powder injection The invention discloses a vincristine freeze-dried powder injection. The vincristine freeze-dried powder injection is made from the following components: 1 g of vincristine, 80 g of dextran, 4-6 g of tartaric acid, and 200 ml of water for injection. The vincristine freeze-dried powder injection provided by the invention is improved in stability, and remarkably prolonged in service life.
EP2102154A1 Water-soluble prodrugs of chloramphenicol, thiamphenicol, and analogs thereof The present invention discloses prodrugs of chloramphenicol, thiamphenicol and their analogs, as well as pharmaceutically acceptable salts thereof, including nitrogen-containing esters of both alcohol groups. These prodrugs have the Formula (I), in which R, Aa, Ll, Mm, Xx, Y and R3 are as defined in the claims. In certain embodiments these prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol, thiamphenicol and their analogs. In one embodiment, a certain subclass of the compounds also possess the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing the active compound in question.
CN103156843A Composition for whitening and removing freckles and preparation thereof The invention provides a composition for whitening and removing freckles. The composition comprises following active components in parts by weight: 1-5 parts of tranexamic acid and 0.5-2 parts of ascorbate, wherein the structural formula of the ascorbate is shown as the specification, wherein R1, R2, R3 and R4 are C10-C20 alkyls; and the alkyls are selected from aromatic hydrocarbon groups and/or aliphatic groups. The composition has good effects of banishing the freckles, removing the freckles and whitening and can be used for chloasma, the freckles, age pigments, aestates and the like, has obvious effect aiming at the chloasma, and is stable and controllable; and meanwhile, an external preparation prepared from the composition provided by the invention can be used for a wounded part, and has fast effect, good curative effect and small toxic or side effect.
US20080161274 Compounds and methods for inhibition of bone loss The invention relates to methods of treating or preventing bone loss, as in osteoporosis, metastatic bone disease, or periodontitis, comprising administering a compound of formula A, a compound of any one of formulae 1-49, a lipoxin compound, or an oxylipin compound.
US20100322971 Method for producing vaccinal viral strain of a virus of the reoviridae family The invention relates to a method for producing a modified viral strain of a virus which is a member of the Reoviridae family and, in particular, relates to vaccinal viral strains of the Orbivirus genus.
CN103340865A Cetirizine hydrochloride tablet and preparation method thereof The invention discloses a cetirizine hydrochloride tablet and a preparation method thereof. The preparation method of the cetirizine hydrochloride tablet comprises the following steps of: dissolving hydroxy propyl cellulose and cetirizine hydrochloride in alcohol, adding blank pellets and slowly adhering the main drug which is coated by the hydroxy propyl cellulose on the surfaces of the pellets in a slow solvent removal process; and uniformly mixing the drug-carrying pellets and pharmaceutically acceptable auxiliary materials and directly tabletting the mixture to form the cetirizine hydrochloride tablet. According to the preparation method of the cetirizine hydrochloride tablet disclosed by the invention, the cetirizine hydrochloride can be prevented from directly contacting with the external environment, so that a preparation device corrosion problem caused by strong drug acidity during a preparation production process can be avoided.
CN102940636A Injection of piperacillin-sulbactum sodium medicine composition and preparation method thereof The invention discloses an injection of a piperacillin-sulbactum sodium medicine composition and a preparation method thereof. The injection disclosed herein comprises 10-15 weight parts of piperacillin, 2.5 weight parts of sulbactam sodium, 2-5 weight parts of lactose, 1 weight part of sodium chloride, and 0.1-0.5 weight parts of sodium citrate. The preparation method comprises the following steps: weighing piperacillin, sulbactam sodium, lactose, and sodium chloride based on the weight parts, using water for injection to dissolve, preparing sodium citrate into a 0.1mol/L solution by using water for injection, adding the 0.1mol/L solution dropwisely to the solution obtained by dissolving and stopping adding dropwisely when the pH value is 6.8, and then dilute with water for injection to make 5000mL to obtain a colorless and transparent medicine solution; filtering the medicine solution by a filtering membrane, drying, conducting sterile crushing, and filling to obtain the injection. According to the invention, the injection has the advantages of good stability, fast dissolving speed, etc.; and the preparation method has simple operation, reduces production cost, and is suitable for large-scale production.
WO2014005968A1 Novel adamantyl derivatives as cannabinoid receptor 2 agonists The invention relates to a compound of formula (I), wherein i.a. A1is -CH2- or -C(O)-; one of R1 and R2 is hydrogen and the other one is -A2 -C(O)-R3; A2 is NH- or absent; and R3 is (A), (B) or (C) The compounds are preferential agonists of the cannabinoid receptor 2 (CB2) and can be used as medicaments for the treatment of pain, inflammation, ischemia, etc.
US20080015251 Means and method for treating lipotoxicity and other metabolically related phenomena A method for treating symptoms of a lipotoxicity-related phenomenon includes introducing into a patient a therapeutically effective synergistic amount of a phenomenon-inhibiting cocktail of a polyphenol (P), thiol antioxidant (To) and ascorbic acid (A) to reduce intracellular reactive oxygen species (ROS) and/or increase intracellular nitrite (NO), so that reduction of such phenomenon is at least 30% greater than the reduction of such phenomenon provided by separate administration of each of P, To and A.
US7666639 Plant deoxyribonucleoside kinase enzymes and their use This invention relates to pharmaceutical compositions comprising plant deoxyribonucleoside kinase enzymes (dNK) capable of phosphorylating nucleoside analogs and to medical use of said dNKs. More specifically the invention relates to the medical use of deoxyribonucleoside kinase enzymes derived from (Arabidopsis thaliana), from loblolly pine (Pinus taeda), from tomato (Lycopersicum esculentum), from maize (Zea mays) or from rice (Oryza sativa). The invention also relates to methods of sensitizing cells to prodrugs, and to methods of inhibiting pathogenic agents in warm-blooded animals using said plant dNKs. In another aspect the invention relates to plant derived deoxyribonucleoside kinase enzymes provided in isolated form from loblolly pine (Pinus taeda), from tomato (Lycopersicum esculentum), from maize (Zea mays) or from rice (Oryza sativa). In further aspects the invention provides polynucleotides encoding the plant dNKs, vector constructs comprising the polynucleotide, packaging cell lines capable of producing said vector, and genetically modified isolated host cells transduced/transfected/-transformed with the vector.
WO2009115534A1 Process for the preparation of 2-amino-2- [2- (4-c3-c21-alkyl-phenyl)ethyl] propane-1, 3-diols The present invention relates to improved processes for the production of 2-amino-2-[2-(4- C2-20-alkyl-phenyl)ethyl]propane-1,3-diols, and to compounds for use therein.
CN103385901A Powder directly used in nasal washing The invention discloses a powder directly used in nasal washing. According to the invention, a soluble substance is extracted according to 0.5g of ginseng, 2g of milk powder prepared by using milk, 4g of granulated sugar, 2g of edible salt, and a proper amount of sorbic acid are fused, crushed, sterilized, bagged, and sealed. 8g per bag of powder is dissolved in 500g of warm water. When the product is used in nasal wash, a user breathes in and out the warm liquid in a bowl several times by using his nose, and breathes in the liquid into the throat and spills out the liquid from the mouth several times; the user breathes in the water, and pinches the nose by using fingers; the user rises his head, and pinches the nose by using fingers and releases the nose several times; the user lowers his head, and the liquid is breathed out; and the user repeats the actions several times. The medicine warm liquid is directly used in nasal wash. With the liquid, dust and bacteria in nasal cavity can be removed in time.
CN1524579B Composite viscoelastic preparation A composite viscoelastic agent for ophthalmology and surgical operation, wherein medicine propagated from eradiating and suppressing cells or promoting cell release from abjunction is used as effective constituent, medicament having color and fluorescence is used as the indicating constituent, the slow release or limitation medicinal diffusing viscoelastic is used as component for mixing. The viscoelastic agent possesses slow release property, viscoelasticity, pseudoplastic behavior and low screening characteristics, and is mainly used for target direction prevention and cure for after-cataract.
CN102232927A Vincristine-PEG-PLGA segmented copolymer nanoparticle, its preparation method and use The invention provides a vincristine-PEG-PLGA segmented copolymer nanoparticle for incorporating vincristine into PEG-PLGA segmented copolymer, also provides a method for preparing the nanoparticle by emulsification-solvent evaporation method and other methods, and use of the nanoparticle in preparing anticancer drug. The nanoparticle provided by the invention can improve the solubility of drugs effectively; can avoid dose dumping and incomplete release to allow the drug to release slowly; can reduce the abilities of RES to identificate and phagocytose nanoparticle, so as to realize the targeted release of the drug in tissues and organs out of the reticuloendothelial system; can reduce toxic and side effect, increase biocompatibility, prolong the circulation time of the drug in the blood; and can increase the compliance of the patients.
CN101342273B Medicament for preventing and controlling botryomycosis of chicken The present invention discloses a medicine which is used for preventing and treating staphylococcus of chicken. The ingredients of the medicine has the following weight portions: 5 to 20 portions of bark of boxthorn root, 5 to 20 portions of Chinese pulsatilla, 5 to 20 portions of Shikonin, 5 to 20 portions of cineole, 5 to 20 portions of corktree, 5 to 20 portions of Jin Qiao Mai (Fagopyrum cymosum (Trey.) Meisn.) , 3 to 12 portions of radix scutellariae, 3 to 12 portions of gentiana scabra bge, 3 to 12 portions of Chinese violet, 3 to 12 portions of diluteyellow crotalaria herb, 3 to 12 portions of madder, 2 to 6 portions of fructus schizandrae, 2 to 6 portions of bark of pomegranate, 2 to 6 portions of Asiatic plantain seed, 2 to 6 portions of alum, 2 to 6 portions of coked rhubarb, and 2 to 6 portions of licorice. The herbs are insolated, weighed, crushed, filtered by a sieve with 60 to 80 meshes, and mixed well, so as to prepare the medicine. When in clinical use, the medicine isdipped for 30 to 60 minutes in boiling water, so that the effective ingredients can be fully dissolved and separated to facilitate the absorption in the body of the sick chicken. Simultaneously, a small amount of sugar and Vc are added to improve the medicinal effects. The medicine has high cure rate, no adverse reaction, no drug-resistance, and no potential of drug residues in the body. The production of the medicine has the advantages of easily accessible raw materials, simple preparation, convenient use, and capability of wide promotion and application in the chicken breeding industry.
WO2006096807A1 Aza-bridged-bicyclic amino acid derivatives as alpha 4 integrin antagonists The invention is directed to aza-bridged-bicyclic compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds are useful α4 integrin receptor antagonists and, in particular, α4β1 and α4β7 integrin receptor antagonists. The invention is further directed to methods for use of the instant compounds for treating integrin mediated disorders including, but not limited to, inflammatory disorders, autoimmune disorders and cell proliferative disorders, methods for preparing the compounds and methods for preparing the intermediates, derivatives and pharmaceutical compositions thereof.
US6967020 Oxygen carrier system, artificial oxygen carrier, and reducing agent An oxygen carrier system includes an artificial oxygen carrier including hemoglobin vesicles encapsulating hemoglobin and an intermediate electron mediator having a standard electrode potential of 0.05 V to 0.56 V (vs. the standard hydrogen electrode) in the vesicles, and a reducing agent which is added to an external aqueous phase of the hemoglobin vesicle to reduce methemoglobin when the hemoglobin encapsulated in the hemoglobin vesicle is oxidized to the methemoglobin. The reducing agent has, as an active component, at least one compound selected from the group consisting of a thiol compound and a reducing sugar.
US20100280077 Process for Preparation of Stable Amorphous R-Lansoprazole A process for preparing stable amorphous R-(+)-lansoprazole comprising optically resolving racemic lansoprazole by the formation of host-guest inclusion complexes by selectively and reversibly including chiral guest molecules in the lansoprazole.
CN103232439A N-heterocyclic methyl tetrahydropyridine-5-substituted indole and preparation method and application thereof The invention discloses a N-heterocyclic methyl tetrahydropyridine-5-substituted indole and preparation method and application thereof, and the structure is shown in the general formula (I): heterocyclic methylamine and methyl acrylate are raw materials, and an intermediate N-heterocyclic methyl-4-piperidone is obtained by three steps of reaction such as Michael addition, Dieckmann condensation and hydrolysis decarboxylation or the like in sequence, and the object (I) is obtained by condensation reaction of the intermediate and 5-substituted indole. The compound (I) can effectively inhibit propagation of cell lines such as human leukemia K562, Jurkat, U937, THP-1; human esophagus cancer ECA-109; human liver cancer SMMC-7721; human ovary cancer HO-8910; human breast cancer MCF-7 and breast cancer MDA-MB-231; the compound inhibits the propagation of cancer cells by promoting cancer cell apoptosis. The compound can be applied to preparation of anticancer medicament.
WO2008119571A2 Nucleic acid myostatin antagonist aptamers obtained by (mirror- image) selex Myostatin antagonists are used to treat muscular generative disorders, type 2 diabetes or obesity. The antanogists are nucleic acid molecules capable of binding to myostatin.
CN103735573A External spray for treating scorpion drying disease The invention provides an external spray for treating scorpion drying disease, and relates to the technical field of culture of special species. The external spray comprises the following components in parts by weight: 0.5-2 parts of rhubarb soda tablets, 1-3 parts of edible salt, and 300-500 parts of purified water. The external spray for treating scorpion drying disease is reasonable in compatibility, remarkable in effect for treating scorpion drying disease, and is easy and convenient to administrate, and low in treatment cost.
CN103520174A Application of compound in preparing medicine for treating bile duct cancer The invention discloses an application of a compound in preparing medicine for treating the bile duct cancer and belongs to the technical field of medicine novel applications. The compound is Asperterpenols A. According to the application of the compound in preparing the medicine for treating the bile duct cancer, in-vitro MTT antineoplastic activity evaluation shows that the Asperterpenols A has the obvious inhibiting effect on growth of human bile duct cell strains RBE, and therefore the Asperterpenols A can be used for preparing the medicine for treating the bile duct cancer and is good in development and application prospect. The application of the Asperterpenols A in preparing the medicine for treating the bile duct cancer is disclosed for the first time, the bile duct cancer cell inhibitory activity of the Asperterpenols A is high, and the application has remarkable progress.
CN1579492A Resina draconis and its total flavone solution preparation and its preparation method The invention discloses a dragon's blood and flavone solution preparations and its manufacturing method. It solves the problem that the normal preparation only uses the dragon's blood powder, and it upgrades the curative effect of dragon's blood, and reduces the loss in external use, reduces the stimulation of the dragon's blood particles. It produces solution type dragon's blood through polyethylene glycol solution, phospholipids and other compound solutions, the weight proportion of the polyethylene glycol solution and the medicine is 1:2-100:1, the polyethylene glycol is the one with molecular of 200-6000. The technology can be produced into solution soft capsule (including intestine dissolution type and colon target direction type), hard capsule solution (including intestine dissolution type and colon target direction type), solution and plaster and injection solution and so on.
CN101954091A Reducible and degradable polymer pre-medicament and preparation method thereof The invention relates to a reducible and degradable polymer pre-medicament and a preparation method thereof, and belongs to the field of biomedical technology and nanomedical technology. The reducible and degradable polymer pre-medicament is characterized in that the structural general formula is MPEG-grafted-SS-PAA-T, wherein MPEG is polyethylene glycol monomethyl ether having a molecular weight of 475 to 5,000Da; SS-PAA is disulfide bond-containing polycystamine; and T is medicinal molecules. The method has the advantages of high efficiency, safety and simplicity.
CN103478710A L-carnitine micro-capsule powder and preparation method thereof The invention relates to L-carnitine micro-capsule powder and a preparation method of the L-carnitine micro-capsule powder. The L-carnitine micro-capsule powder comprises L-carnitine, maltodextrin, Arabic gum, gelatin and sodium ascorbate. The preparation method comprises the following steps: (1) weighing 5wt% of gelatin, adding the gelatin into water and swelling for about 1 hour, heating to 45 DEG C, stirring till the gelatin is fully dissolved, then adding 4wt% of Arabic gum and 4wt% of maltodextrin to the gelatin liquor, stirring for dissolving, and finally obtaining packing material liquor; (2) adding 85wt% of L-carnitine, 1wt% of sodium ascorbate and 1wt% of tricalcium phosphate into the packing material liquor, stirring to fully dissolve, and uniformly mixing to obtain an embedding liquid; and (3) spraying and drying the embedding liquid by a spray drying tower to obtain the microencapsulated L-carnitine powder. According to the L-carnitine micro-capsule powder and the preparation method of the L-carnitine micro-capsule powder, the L-carnitine with strong water absorption characteristic is embedded by the packing material, so that the stability of the L-carnitine is enhanced. Furthermore, the preparation method is greener and more environment-friendly.
US20100028326 Diagnosis of hyperinsulinemia and type ii diabetes and protection against same based on proteins differentially expressed in serum Mouse proteins differentially expressed in serum, in comparisons of normal vs. hyperinsulinemic, hyperinsulinemic vs. type 2 diabetic, and normal vs. type 2 diabetic white adipose tissue have been identified, as have corresponding human proteins. The human molecules, or antagonists thereof, may be used for protection against hyperinsulinemia or type 2 diabetes, or their sequalae.
WO2009093018A1 New use for cannabinoids The present invention relates to the use of CBD alone or in combination with another cannabinoid, in the manufacture of a pharmaceutical or neutraceutical formulation for use in controlling cholesterol levels in a subject. It also relates to the use of THCV alone or in combination with another cannabinoid, in the manufacture of a pharmaceutical or neutraceutical formulation for use in increasing energy expenditure in a subject. Furthermore the CBD alone or in combination with another cannabinoid or the THCV alone or in combination with another cannabinoid are used as part of a regime to manage or treat type I or II diabetes, obesity, dyslipidaemia, related metabolic disorders and cardiovascular disease.
CN103565789A Application of galangin in preparation of anti-tumour metastasis medicine The invention belongs to the field of natural medicines and in particular discloses application of galangin in inhibition of transcription and expression of an FAK (focal adhesion kinase) gene, inhibition of functions of FAK through phosphorylation, inhibition of cell adhesion, infiltration and migration and inhibition of tumour metastasis. The invention also relates to a galangin medicine prepared by adopting the conventional medicine preparation method, galangin can be combined with the conventional tumour treatment medicine and treatment method when being used, and treatment application is carried out by adopting the conventional oral, intravenous and intraperitoneal administration routes, so that a foundation is laid for further application of the galangin.
US20130116203 Isothiocynates and glucosinolate compounds and anti-tumor compositions containing same The present invention provides glucosinolate and isothiocyanate compounds and related methods for synthesizing these compounds and analogs. In certain embodiments, these glucosinolate and isothiocyanate compounds are useful and chemopreventive and or chemotherapeutic agents.
EP2070519A1 Preparation for the prevention and/or treatment of dementia syndromes The present invention relates to a preparation suitable for the prevention and/or treatment of vascular disorders, comprising the following fractions: fraction a) long chain polyunsaturated fatty acids; fraction b) phospholipids, which fraction contains at least two different phospholipids selected from the group consisting ofphosphatidylserine, phosphatidylinositol, phosphatidylcholine and phosphatidylethanolamine. fraction c) compounds which are a factor in methionine metabolism, which fraction contains at least one member selected from the group consisting of folic acid, vitamin B12, vitamin B6, magnesium and zinc.
US20110165633 Production of Polyketides and Other Natural Products The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential use of novel FKBP-ligand analogues and host cells that produce these compounds. The invention is particularly concerned with methods for the efficient transformation of strains that produce FKBP analogues and recombinant cells in which cloned genes or gene cassettes are expressed to generate novel compounds such as polyketide (especially rapamycin) FKBP-ligand analogues, and to processes for their preparation, and to means employed therein (e.g. nucleic acids, vectors, gene cassettes and genetically modified strains).
WO2013139734A1 Use of (rs)-s-cyclopropyl-s-(4-{[4-{[1r, 2r)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide for treating specific tumours The invention relates to the use of (R)-S-cyclopropyl-S-(4-{[4-{[(1R, 2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide and/or (S)-S-cyclopropyl-S-(4-{[4-{[(1R, 2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2- yl]amino}phenyl)sulfoximide for treating specific tumours.
WO2009126737A2 Triterpene saponins, methods of synthesis, and uses thereof The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.
CN103040857A Application of phyllanthus urinaria polysaccharide component in preparing drug for resisting hepatitis B virus The invention relates to an application of a phyllanthus urinaria polysaccharide component in preparing a drug for resisting a hepatitis B virus, and belongs to the field of medicine. The phyllanthus urinaria polysaccharide component is a phyllanthus urinaria polysaccharide component PUIP II which comprises rhamnose, arabinose, mannose and glucose at a molar ratio of 0.11:0.36:0.08:0.45. The phyllanthus urinaria polysaccharide component is artificially extracted, separated and purified by a medicinal plant, namely phyllanthus urinaria. An in-vitro bioactivity experiment indicates that the phyllanthus urinaria polysaccharide component PUIP II can inhibit secretion of HBsAg and HBeAg and reproduction of HBV-DNA (hepatitis B virus-deoxyribose nucleic acid) in HepG2.2.2.15 cell culture, and has a certain in-vitro HBV activity resistance effect, and an in-vivo activity experiment indicates that the PUIP II has an obvious inhibiting effect on DHBVDNA (duck hepatitis B virus deoxyribose nucleic acid) in a duck, is smaller in bounce, and can be used for preparing the drug for resisting the hepatitis B virus and for preparing health care products for protecting a liver.
WO2012122707A1 Quaternary ammonium salt compounds, preparation method, pharmaceutical composition and use thereof Quaternary ammonium salt compounds of general formula (I), the preparation method thereof, the pharmaceutical composition comprising compounds as the active components, and the use of compounds in the preparation of medicaments for treating diseases associated with Lp-PLA2 enzymic activity are provided in the present invention. In general formula (I), R1, R2, R3 are independently C1-4 alkyl, or R1 is C1-4 alkyl, R2 and R3 are taken together to form C4-5 alkylidene groups, X is F, Cl, Br or I.
CN101757613A Medicine for preventing and treating canine viral disease The invention relates to compound medicine for preventing and treating canine viral disease, which comprises the following main components: poly IC and interferon. The medicine of the invention can stimulate an organism to keep producing interferon while treating the disease so as to form a continuous treatment process and achieve the purpose of thoroughly curing the disease. Two types of medicine interact to effectively treat virus diseases, enhance the resistance of the organism, and realize the effect of preventing the occurrence of the diseases and avoiding secondary infection.
US20050080041 Method and composition for the treatment of adenoviral ocular infections Adenoviral infections and in particular ocular adenoviral infections, e.g. kerato-conjunctivitis, can be treated or alleviated by the administration of a substance, interfering with the interaction between the virus and the sialic acid receptor, in a therapeutically effective amount.
US20100004231 Inhibitors of burton's tyrosine kinase This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2′, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
WO2009137044A2 Inhibitory effects of nordihydroguaiaretic acid (ndga) on the igf-1 receptor and androgen dependent growth of lapc-4 prostate cancer cells Disclosed herein are methods and compositions for the treatment of prostate cancer with an IGF-1 receptor kinase inhibitor. Methods are also provided for the treatment of prostate cancer by identifying a level of IGF-1 receptor expression and making a decision whether to treat with an IGF-1 receptor kinase inhibitor.
WO2014058801A1 2'-chloro nucleoside analogs for hcv infection Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2'-chloro nucleosides according to Formula 2001: (2001); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.
US20080070913 Thieno [ 3,2-b] pyridine-6-carbonitriles and thieno [2,3-b] pyridine-5-carbonitriles as protein kinase inhibitors This invention provides compounds of Formula (1a)-(1f), II wherein: X, m, n, q, R1, R2, R3, R4, R5, R6, R7, R8, R9, Y, Q, Z, Z′, Z′″, Z″ and J are defined hereinbefore in the specification, which are useful in the treatment of cancer, stroke, myocardial infarction, neuropathic pain, osteoporosis, polycystic kidney disease, autoimmune disease, rheumatoid arthritis, and transplant rejection and process for producing said compounds.
CN102643278A Pyrrolo[2,3-d]pyrimidine derivative and application in preparation of anti-malignant tumor medicament thereof The invention relates to a novel pyrrolo[2,3-d]pyrimidine derivative and an application in preparation of anti-malignant tumor medicaments thereof. The pyrrolo-pyrimidine compound of the invention is an ideal folic acid-dependent enzyme inhibitor, and has the advantages of less first-pass effect, high effective bioavailability, few dosage, less side effect, and the like when used for the prevention or treatment of various tumors such as leukemia, breast cancers, lung cancers, pancreas cancers, bladder cancers, stomach cancers, mesothelial cancers, colorectal cancers, and the like.
CN103656104A Application medicine for treating chronic fatigue syndrome and preparation method thereof The invention provides an application medicine for treating chronic fatigue syndrome and a preparation method thereof. The method comprises the following steps: crushing morinda officinalis, fructus cnidii, dodder, ephedra, angelica root, herba epimedii, asarum, borneol and semen allii tuberose into medicinal powder; adding lanolin, and uniformly regulating with water to prepare an ointment product which is used for treating chronic fatigue syndrome through acupoint application. The medicine has the functions of warming yang and tonifying qi, and supporting and tonifying kidney, is suitable for spleen and kidney deficient patients with chronic fatigue syndrome, is convenient to use and exact in curative effect, and does not have toxic or side effect. Clinical curative effect observation indicates that the total effective rate of the application medicine is 92.59 percent.
WO2007028456A1 Substituted pyridocarboxamides as inhibitors of plasminogen activator inhibitor 1 (pai-1) The invention relates to substituted pyridocarboxamides, to a process for preparing them and to their use for producing medicaments for the treatment and/or prophylaxis of diseases in humans and animals, particularly of thrombotic disorders.
WO2013167514A1 New 2,3-dihydro-furo[2,3-c]pyridines, their use as modulators of the g-protein-coupled receptor gpr119 and pharmaceutical compositions comprising them The present invention relates to compounds of general formula I, wherein the groups R1 and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
CN102816159A Alpha-mangostin thiazole formate A, as well as semi-synthesis method and pharmaceutical application thereof The invention relates to a new compound which is prepared through esterification reaction of alpha-mangostin and thiazole-2-formic acid used as a raw material in the presence of a catalyst, has the chemical name of 7-methoxy-2,8-2-(3-methyl-butyrate-2-alkene) di-benzene pyrrone-1,3,6-tri(thiazole-2-formic acid) ester, and is called alpha-mangostin thiazole formate A for short. The yield of the alpha-mangostin thiazole formate A is more than 80%. The alpha-mangostin thiazole formate A can be widely applied in the preparation of antineoplastic medicines.
US7118750 Modified TNF-alpha molecules, DNA encoding such and vaccines comprising such modified TNF-alpha and DNA A modified human TNFα molecule is capable of raising neutralizing antibodies towards unmodified human TNFα following administration of the modified TNFα to a human host, wherein one or more peptide fragments of the human TNFα molecule has been substituted by one or more peptides containing immunodominant T cell epitopes or a truncated form of the molecule containing the immunodominant epitope and one or both flanking regions of the human TNFα-molecule containing at least one TNFα B cell epitope, wherein the substitution introduces a substantial change in the amino acid sequence of any one of the strands of the front β-sheet, in any one of the connecting loops, or in any one of the B′, I, or D strands of the back β-sheet.
US20050136113 Dosage form comprising a semipermeable wall defining a cavity having an exit orifice; expandable layer; flow control agent; sustained release push delivery devices having high drug loading with minimized residue Controlled release of active agents from sustained release push delivery devices having high drug loading are described wherein residual drug content in the device is minimized by the utilization of a flow-promoting layer between a semi-permeable wall and drug layer comprising the device.
WO2008016139A1 Fluorescent oleamide derivative and use thereof An oleamide can emit fluorescence without largely deteriorating its biological activity by introducing a fluorescent group into the oleamide via a carbon chain, as shown in the formula (I). The fluorescent group (R) may be a dansyl group of the formula (II) or an NBD group of the formula (III). The compound is useful for any application such as a method for fluorescence observation of a cell, a gap binding inhibitor, a tool for the study of the intracellular action mechanism of an oleamide derivative, a pharmaceutical product, a food, a beverage and a supplement.
US20120115941 Compounds Affecting Glycemic Index Compounds of formula I are disclosed which are useful as glycemic index lowering agents and/or, as α-amylase and/or α-glucosidase inhibitors. Also disclosed are nutritional and/or pharmaceutical compositions and supplements comprising one or more of these compounds. The compounds will be beneficial to patients who require stabilization of their postprandial glucose levels.
CN102574843A Fused ring analogues of anti-fibrotic agents The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
WO2009001551A1 Regulator of activity of bone-forming protein Disclosed is a composition which can regulate the activity of a bone-forming protein involved in the formation of a bone tissue or a cartilage tissue. Specifically disclosed are: a regulator of the activity of a bone-forming protein, which comprises a sulfated galactosaminoglycan having 0.6 piece or more ester sulfate group on average per one constituent monosaccharide or a salt thereof as an active ingredient; and a composition comprising a sulfated galactosaminoglycan having 0.6 piece or more ester sulfate group on average per one constituent monosaccharide or a salt thereof and BMP-2, BMP-3, BMP-4, BMP-5, BMP-6, BMP-7, BMP-8, BMP-9, BMP-10, BMP-11, BMP-12, BMP-13, BMP-14 and/or BMP-15.
US7208518 antiinflammatory agents; asthma; 2-hydroxy-3-(4-hydroxy-5-methyl-2-oxo-2H-chromene-3-yl)-9-methyl-2,3-dihydro-4H-furo[3,2-c]chromene-4-one; from 4-Hydroxycoumarin and glyoxal The present invention relates to novel compounds of the formula (I) including all stereoisomers and tautomers thereof, to the pharmaceutically acceptable salts and solvates thereof, to the processes and reactive intermediates for their preparation and to their use in the prophylaxis and treatment of asthma and other inflammatory diseases and/or conditions in humans.
CN101347590A Composition for treating postpartum diarrhea, promote digestion and eliminate indigestion, and method for producing the same The invention relates to an assembly formula for treating post partum diarrhea, helping digestion and relieving oppression and a manufacturing method thereof, wherein, the assembly formula takes drug ingredients such as walnut, Chinese date, propolis, honey, brown sugar, black alum, hernial sac, oberthuria daxidi, amomum villosum, safflower, radix aucklandiae, balloon flower and dandelion as raw materials. In order to ensure masses of patients who have intestines and stomach diseases obtains more ideal treating medicine, the invention provides the assembly formula used for simultaneously treating post partum diarrhea, helping digestion and relieving oppression and the manufacturing method thereof; the assembled medicine can be used for treating post partum diarrhea which can not be effected a radical cure for a long time, helping digestion and relieving oppression; furthermore, the formula is reasonable; the manufacturing technique is easy to operation, and the medicine can be afforded by the masses of patients.
DE102006045389A1 Topically acting dermatological humectant comprises hyaluronic acid and panthenol in the multilamellar layers of hydrogenated liposomes Topically acting dermatological humectant comprises hyaluronic acid (0.1-1 wt.%) and panthenol (5-50 wt.%) in the multilamellar layers of hydrogenated liposomes (5-50 wt.%), together with water, solubilizer and cosmetic ingredients. An independent claim is also included for producing a topically acting dermatological humectant by preparing a mixture of hydrogenated liposomes, hyaluronic acid, pathenol and optionally water and additives at 90-110[deg] C and subjecting the mixture to high-pressure homogenization.
WO2010027040A1 HAIR GROWTH PROMOTING AGENT CONTAINING 15,15-DIFLUOROPROSTAGLANDIN F2α DERIVATIVE AS ACTIVE INGREDIENT Provided is novel medicinal use of a 15,15-difluoroprostaglandin F2α derivative. As a result of intensive studies in order to discover novel medicinal use of a 15,15-difluoroprostaglandin F2α derivative, it was found that, in Phase III clinical trial in Europe of tafluprost which is a 15,15-difluoroprostaglandin F2α derivative with patients with open-angle glaucoma or ocular hypertension, tafluprost has actions of growing eyelashes, making eyelashes thick and changing the color thereof, that is, has an effect of promoting the growth of hair (eyelashes). Therefore, a 15,15-difluoroprostaglandin F2α derivative is useful as a hair growth promoting agent, and is expected to be useful as an active ingredient of a preventive or therapeutic agent for a disease associated with hair such as alopecia and a hair care product or a hair cosmetic product for hair regrowth, hair growth, increase in hair density, hair pilatory, etc.
US20120190708 Targeting nad biosynthesis in bacterial pathogens The emergence of multidrug-resistant pathogens necessitates the search for new antibiotics acting on previously unexplored targets. Nicotinate mononucleotide adenylyltransferase of the NadD family, an essential enzyme of NAD biosynthesis in most bacteria, was selected as a target for structure-based inhibitor development. To this end, the inventors have identified small molecule compounds that inhibit bacterial target enzymes by interacting with a novel inhibitory binding site on the enzyme while having no effect on functionally equivalent human enzymes.
WO2011104490A3 Use of essential oil of oregano or of rosewood for the treatment of cancerous keratoses The present invention relates to various compositions comprising essential oil of Origanum compactum or of Aniba rosaeodora, or a constituent thereof, preferably a majority constituent, for use in the targeted treatment and the prevention of keratoses in the transformation phase and of carcinomas resulting from these keratoses, and more particularly of keratoses induced by solar radiation on the skin of an individual. The present invention relates most particularly to compositions based on the essential oil of oregano or of rosewood, or else on linalol, thymol or carvacrol.
CN103446126A Application of Lycojaponicumin B in anti-herpes virus drug The invention discloses application of Lycojaponicumin B in preparation of an anti-herpes virus drug. An experiment proves that the Lycojaponicumin B has remarkable inhabiting effect on Herpessimplexvirus 1 (HSV-1) and Herpessimplexvirus 2 (HSV-2) and has potential application value in the field of treatment of herpes virus infectious diseases. An experimental basis is provided for the Lycojaponicumin B in clinic treatment of the herpes virus infectious diseases, and the Lycojaponicumin B has certain guiding significance on development of anti-HSV-1 and anti-HSV-2 drugs and important reference value.
CN103494985A Externally applied patch for treating gynecological myoma of uterus and ovarian cyst The invention discloses an externally applied patch for treating gynecological myoma of uterus and ovarian cyst. The externally applied patch consists of marmor serpentinatum, sulfur, clove, cinnamon, radix angelicae, Astragalus membranaceus, frankincense, myrrh, fennel, rheum officinale, Chinese blister beetles, Sargassum, selfheal, dragon's blood, crude sichuan aconite roots, radix aconite, white spirit, rice vinegar and active carbon iron powder. Most of the medicinal raw materials of the patch are yang-warming medicines. Medicines for promoting blood circulation to remove blood stasis can improve microcirculation, increase the blood flow volume, change the rheological property of blood and promote obsolete bleeding absorption in mesometrium without envelope. Medicines for softening hardness and transforming phlegm can promote macrophage proliferation and release of connective tissues, so that proliferous fiber cyst in the mesometrium is softened. Aiming at etiology and pathogenesis of the symptoms, the externally applied patch disclosed by the invention warms and invigorates kidney yang, disperses blood stasis, tonifies qi and yang and warms kidneys without the deficiency of improving too much yang to cause heat. As the patch directly reaches focuses and is quickly transdermal, so as to take effect quickly. The effective components of the medicines directly reach the focuses.
US20120178813 Lipid-lowering antidiabetic agent A composition which includes a salt of metformin and the use of the composition for treatment of or use in prediabetes, diabetes, lowering triglycerides and/or other conditions in mammals.
CA2696767A1 Heterocyclic amides useful for the treatment of cancer and psoriasis The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2 or R3 is (Z).
US20050107611 For use as adenosine receptor ligands; immunostimulants; contraceptives The invention relates to derivatives of the pyrazoyl[1,2,4]triazolo[4,3-α]quinoxaline according to formula (1), or of its analog in the form of the pyrazolyl-substituted tetrazolo[1,5-α]quinoxalines according to formula (2). The substances according to formula 1 or 2, in this form or in the form of their pharmaceutically acceptable salts, are suitable as active agents, especially as adenosine receptor ligands.
WO2008084492A1 5-(heterocyclyl)alkyl-n-(arylsulfonyl)indole compounds and their use as 5-ht6 ligands The present invention relates to novel 5-(Heterocyclyl)alkyl-N- (arylsulfonyl)indole compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardiovascular diseases and cancer.
CN102114017A Medicinal composition containing amlodipine and perindopril and application thereof The invention relates to a novel medicinal composition. The medicinal composition consists of 1-40mg of perindopril or pharmaceutically acceptable salt or ester of the perindopril, and 0.3-20mg of amlodipine or pharmaceutically acceptable salt or ester of the amlodipine and pharmaceutically acceptable vector, wherein the perindopril or the pharmaceutically acceptable salt or ester of the perindopril is perindopril tert-butylamine salt or perindopril arginine; and the amlodipine or pharmaceutically acceptable salt or ester of the amlodipine is amlodipine maleate, amlodipine mesylate, L-amlodipine aspartate, amlodipine camphor sulfonic acid, amlodipine camsylate, amlodipine nicotinate, amlodipine pyroglutamate or levoamlodipine besylate. The medicinal composition is used for preventing, retarding or treating hypertension and related diseases of patients, so the incidence rate and/or death rate of heart cerebrovascular diseases is reduced, the adverse effects of medicaments are reduced, and the administration compliance of the patients is improved.
CN103736099A Prodrug with nitrophenyl alkyl acid connected with alkaline antitumor drugs and preparation method thereof The invention belongs to the field of molecule targeting system, and particularly relates to a prodrug with nitrophenyl alkyl acid compounds connected with alkaline antitumor drugs. The prodrug of the invention is characterized in that when compared with antitumor drugs, the prodrug enhances the in-vivo stability of antitumor drugs, reduces the toxicity of antitumor drugs to normal tissue, and also has the effect of targeting tumor tissue. The prodrug of the invention has better antitumor activity. The invention also relates to a preparation method and applications of the prodrug. The prodrug of the invention has better in-vivo and in-vitro stability, better effect of targeting tumor hypoxic tissue, and better antitumor effect.
CN103254057A Compounds and pharmaceutical compositions thereof for inhibiting mammalian tumor cell proliferation Compounds of following general formula (I) and pharmaceutical compositions thereof for inhibiting mammalian tumor cell proliferation are disclosed. In formula (I), n is an integer from 0 to 9. The cell proliferation of breast tumor, ovarian tumor, skin tumor or liver tumor is inhibited by the compounds of the formula (I).
CN102085193A Tibolone orally disintegrating tablets and method for preparing same The invention provides tibolone orally disintegrating tablets and a method for preparing the same. The tibolone orally disintegrating tablets comprise tibolone serving as a main ingredient and a disintegrating agent, a bulking agent, a flavoring agent and the like serving as auxiliary ingredients. The preparation method comprises the steps of mixing, direct tabletting, coating and the like. The tibolone orally disintegrating tablets have the formulation advantages that the tablets can be disintegrated or dissolved in the mouth without water and enter the alimentary tract along with the swallowing action, and the in-vivo behavior of the tablets is the same as that of the common tablets. The tibolone orally disintegrating tablets have the characteristics of convenience of taking, rapid absorption, high bioavailability and the like, and can improve the adaptability of patients and offer more options for doctors and patients in clinical administration.
CA2305256C Mometasone furoate suspensions for nebulization An aqueous nebulizer suspension contains water, mometasone furoate monohydrate, a nonionic surfactant, a soluble salt and optionally a pH buffer. The suspension may be prepared by ultrasonication or jet milling techniques.
CN101792399A Aminosalicylic acid derivative lysine complex salt, preparation method and application thereof The invention relates to aminosalicylic acid derivative lysine complex salt, a preparation method and application thereof. The structure of the aminosalicylic acid derivative lysine complex salt conforms to the following general formula (I), R1 stands for -H, -Cl or -Br; R2 stands for -F, -Cl or -Br; one of R3 and R4 stands for COO-, and the other one stands for -OH or -OCOCH3. A target compound of the aminosalicylic acid derivative lysine complex salt has the pharmacological action of treating neuropathic pain.
CN102091046A Fludarabine phosphate freeze-dried powder injection and preparation method thereof The invention belongs to the technical field of medicines, and relates to a fludarabine phosphate freeze-dried powder injection and a preparation method thereof. The fludarabine phosphate freeze-dried powder injection consists of fludarabine phosphate and mannitol in a mass ratio of 1:(0.6-1.2). The method for preparing the fludarabine phosphate freeze-dried powder injection comprises the following steps of: adding water for injection into a liquid preparing tank, adding the fludarabine phosphate in a prescription amount, adding alkali, stirring until the mixture is dissolved completely; and adding the mannitol, regulating the pH value, adding active carbon for decolorizing, filtering for decolorizing, performing fine filtering by using a filter membrane, subpackaging, and performing freeze drying. The fludarabine phosphate freeze-dried powder injection has excellent formability, clarified appearance of solution to be frozen, high redissolution performance of freeze-dried products, high clarity after redissolution, low impurity content and moisture content, high stability and controllable quality.
CN102697960A Medicament for treating recurrent oral ulcer and preparation method thereof The invention discloses a medicament for treating recurrent oral ulcer and a preparation method thereof and belongs to the technical field of medical preparations. According to the technical scheme, the medicament for treating recurrent oral ulcer is prepared from the following active ingredients by mass: 100 to 200mg of keel, 180 to 220mg of pearl, 40 to 80mg of belladonna, 20 to 50mg of calculus bovis, 150 to 200mg of ranitidine, and the balance of 500mg of rock sugar serving as a mouthfeel regulator and 20mg of vitamin C. The medicament can induce astringency and prevent exhaustion, remove toxicity and promote tissue regeneration, resolve tetany and relieve pain, clear away the heart fire, induce resuscitation and expel wind, strengthen immune function of organisms, repair mucosa and timely and effectively promote mucosa healing.
CN102526759A Dendritic-polymer-based high-bioavailability oral puerarin preparation The invention relates to a dendritic-polymer-based high-bioavailability oral puerarin preparation, which is characterized by being prepared from a composite formed by polyamide-amine dendritic polymers of the second generation (G2) and medicines. Compared with the conventional puerarin oral preparation, the dendritic-polymer-based high-bioavailability oral puerarin preparation has the advantage that the oral bioavailability of puerarin is improved obviously. The puerarin oral preparation can be prepared into liquid solutions and solid tablets or capsules.
CN101810574A Method for preparing stable docetaxel submicron emulsion injection and freeze-dried emulsion The invention discloses a method for preparing stable and high drug-loading rate intravenous docetaxel submicron emulsion injection and freeze-dried emulsion. A main active ingredient of the submicron emulsion is docetaxel, and the auxiliary materials are oil for injection, an emulsifying agent, a stabilizing agent, an isoosmotic adjusting agent, lyoprotectants and water for injection. The docetaxel content is 1 to 10mg/ml. The emulsion has small grain size, and the grain size range after the submicron emulsion injection and the freeze-dried emulsion are dissolved compositely is 100 to 200nm. By selecting proper oil phase and emulsifying agent to optimize the preparation process, the prepared docetaxel submicron emulsion injection and freeze-dried emulsion have the characteristics of high drug-loading rate, high stability, easy industrial production, strong clinical applicability and the like.
US20120277197 Tigecycline formulations The invention is directed to a frozen pharmaceutical formulation suitable for administration to a subject parenterally, comprising a therapeutically effective amount of tigecycline and an agent selected from the group consisting of lactose, dextrose, glucose, mannose, sucrose, ribose, xylose and a combination thereof, wherein the formulation in a pre-frozen state at about 22° C. or in an unfrozen state at about 22° C. has a pH in the range of from 4.0 to 5.5. Preferably, the formulation is suitable for storage at or below about −20° C. over a period of at least about 2 months, preferably 6 months, more preferably 26 months. Alternatively, the formulation is suitable for storage at about 22° C. over a period of about 24 hours.
EP2402362A2 Crystalline forms of smilagenin The invention provides smilagenin in novel crystalline, hydrated forms, and the use thereof in manufacturing pharmaceutical or edible grade smilagenin and its derivatives.
CA2572529C Dental compositions with sensitivity relief A one-component prescription fluoride treatment composition having both fluoride efficacy and sensitivity relief is disclosed. The composition includes at least one metal fluoride and a nerve desensitizing agent such as potassium nitrate. The invention further includes a composition having at least one metal fluoride comprising from about 4900 ppm to about 5000 ppm of available fluoride; less than about 5 percent by weight of at least one alkali metal salt having desensitizing effect; at least one carrier; and at least one foaming agent that has thickening property. The composition may be formulated into a gel, a paste or any other convenient form, some of which contain abrasives.
WO2006082371A1 Pyrimidine compounds having tie2 (tek) inhibitory activity The invention relates to a compound of the Formula (I) or salt, prodrug or solvate thereof, wherein Rx, Ry, Rz, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm blooded animal. The invention also relates to processes for the preparation of said compounds.
US20090042969 Use of Specific Trifluoromethyl Ketones for Preventing and Treating Pancreatitis The present invention relates to the use of specific trifluoromethyl ketones for preventing and treating pancreatitis and, more particularly, chronic pancreatitis or chronically recurring pancreatitis.
CN103120687A Application of Eryngiolide A in medicine for resisting tubercle bacillus The invention discloses an application of Eryngiolide A in preparation of a medicine for resisting tubercle bacillus. The Eryngiolide A has outstanding inhibitory activity on the tubercle bacillus and very good application prospect by aiming at the existing conditions that current tuberculosis morbidity is high and tuberculosis morbidity and mortality shows a rising trend due to the generation of multiple mycobacterium tuberculosis medicine-resistant strains. The application of the Eryngiolide A in preparation of the medicine for resisting the tubercle bacillus is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Eryngiolide A on the tubercle bacillus is inconceivably high; and the Eryngiolide A has outstanding substantiality characteristic without possibility of any inspiration given by other compounds and obviously achieves the outstanding progress by being used for preventing and treating tubercle bacillus infection.
CN1923837A Lipophilic platinum antineoplastic complex The invention discloses a new-typed complex of platinum, which is characterized by the following: adopting cis-[PtA2I2](A2 is carrier group 1R, 2R-cyclic hexamethylene or 2-isopropyl-(4R,5R)-4,5-di(aminomethyl-1, 3-dioxocyclopentane) as raw material; reacting with silver nitrate in the water quantitatively; filtering to separate Agl; adding 3-isopropyl-5-methyl salicylic acid or 3, 5-sodium diiodosalicylate salt in the mother liquid; purifying.
CA2544731A1 Rapamycin peptides conjugates: synthesis and uses thereof The present invention relates to new rapamycin derivatives for the inhibition of cell proliferation. The compounds can advantageously target two proteins in dividing cells and interfere with cell cycle. There is thus provided derivatives of rapamycin in which the 42 position of rapamycin is linked to an amino acid or a peptide through a carbamate ester linkage. These rapamycin derivatives can be synthesized by reacting 42-O-(4-Nitrophenoxycarbonyl) rapamycin and an amino acid or a free amino peptide under basic conditions. These rapamycin derivatives can be used to inhibit the cell cycle and are therefore useful for treating cell proliferation disorders.
WO2014072311A1 Medicament comprising at least one omega-3 polyunsaturated fatty acid A medicament comprising a therapeutically effective amount of at least one omega-3 polyunsaturated fatty acid for use in the reduction and prevention of post-ischemic damages in patients undergoing elective surgery.
WO2013081094A1 Imidazo[1,2-a]pyridine derivative and use thereof for medical purposes The purpose of the present invention is to provide a compound that can act on mGluR5 selectively to inhibit the signaling of mGluR5. The present invention provides an imidazo[1,2-a]pyridine derivative typified by the compound shown below or a pharmacologically acceptable acid addition salt thereof.
EP0991408B1 Novel process for manufacturing paroxetine solid dispersions Solid dispersions of poorly soluble drugs are disclosed which are prepared using a solvent or fusion process. Such dispersions are manufactured with the free base of the drug, specifically paroxetine free base, an oil, allowing for a low temperature for the fusion process, decreased organic solvent volumes for the solvent process and the formation of a paroxetine salt during the solid dispersion manufacture process.
US20080090900 Antibiotic bushrin This invention describes a new antibiotic, hereinafter designated as bushrin, having the formula C16H16O2, which is 7-(3-furyl)-3,7-dimethyl-7,8-dihydro-1-naphthalenol, its production method by fermentation, and the methods related to its recovery, concentration and purification from the crude solutions. The invention includes within its scope the agent in dilute form, as a crude concentrate, and in pure form. The invention also relates to the use of the compound according to the invention in antimicrobial compositions and as antiseptics or disinfectants.
EP1761496A2 Non-imidazole heterocyclic compounds as histamine h3-receptor ligands Certain non-imidazole heterocyclic compounds of formula (I) are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases, wherein in the A- and B-containing ring, I) A, B1 and B2 are CH; II) A is CH, one of B1 and B2 is N, and the other of B1 and B2 is CH; or III) A is absent, B1 is CH, and B2 is O; L is -C1-4alkylene- or a covalent bond; Q is -(CH2)mO-, -(CH2)nC=C-(where the -O- and -C=C-portions are directly attached to the ring), carbonyl, or thiocarbonyl; m I 2, 3, or 4; n is 1, 2, 3, or 4.
US20100249051 Bioactive Molecules from Co-Cultivation of Microbes Certain aspects of the invention relates to antibiotics, as well as pharmaceutically acceptable salts, pro-drugs and/or analogs thereof. Another aspect of the inventions relates to methods of use of said antibiotics.
WO2014100696A1 Nutritional formulations using human milk oligosaccharides for modulating inflammation Disclosed is a nutritional composition for use in modulating or reducing inflammation in an adult or elderly individual in need thereof. In some aspects, the nutritional composition comprises a neutral human milk oligosaccharide.
WO2014102788A1 Foamable otic pharmaceutical compositions The present invention relates to foamable otic pharmaceutical compositions comprising oil-in-water emulsions which comprise an antibiotic agent and a propellant gas. The pharmaceutical compositions are administered to the ear as foam for treating ear disorders.
WO2013004075A1 Tumor targeted drug combretastatin a4 derivative The present invention relates to a group of A-ring 4-position substituted 3,5-dimethoxy phenyl imidazole, oxazole and thiazole tumor targeted drug Combretastatin A4 derivatives, the phosphoric acid ester and sulphonic acid ester thereof, or the pharmaceutically acceptable salt, glycoside derivatives and solvolyte thereof. A pharmacological activity screening test shows that a compound has better exosomatic antitumor activity and good microtubulin inhibition effect.
US20120122887 Solid state forms of a potent hcv inhibitor This invention relates to novel sodium salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:
WO2008105038A1 Adhesive patch for mycosis An adhesive patch for application to a nail and/or the skin for the prevention or treatment of mycosis. It can maintain a high drug concentration in the nail and/or horny layer of the skin for long without the aid of a dissolving agent for preventing drug crystallization/precipitation or an accelerator for accelerating drug penetration into the nail and/or skin. It has excellent adhesion even in long-term wear, and is less irritative to the skin. The adhesive patch, which is for application to a nail and/or the skin for the prevention or treatment of mycosis, comprises an acrylic pressure-sensitive adhesive layer or silicone pressure-sensitive adhesive layer, and the adhesive layer contains an antifungal agent having an octanol-water partition coefficient, logKo/w, of 4 or higher, the antifungal agent being contained in a dissolved state.
US20090069278 Hormonally-timed dermatological preparations This invention provides a dermatological preparation to improve skin cosmesis or conditioning by using different formulations in a sequence that suits the needs of the skin at different points of the hormonal cycle. In its simplest implementation, this would be a two-phase skin treatment, such as a cosmetic, lotion or soap whose formulation changes to balance the differing states of hydration and reactivity of the skin during the early and late phases of the cycle. The formulations would be made in a way to be easily identified and delivered conveniently for use at different times of a hormonal cycle. The preparation would be packaged to permit the convenient purchase and dispensing of the different formulations in a manner that could be easily sequenced with the hormonal cycle.
CN103393982A Nerve calming liquid A nerve calming liquid is composed of honeysuckle flower, Weeping Forsythia, Folium Perillae, mint, cinnabar, Radix et Rhizoma Nardostachyos, Radix Polygalae, Albizia julibrissin, Poria cum Ligno Hospite, longan, Wrinkled Gianthyssop, unprepared rehmannia root, spine date seed, malt and safflower. The nerve calming liquid has a pleasant aroma, scents air, and calms the nerve and mind to realize the auxiliary hypnosis effect. The nerve calming liquid is completely different from 'maze scent' in terms of composition medicines, is a sleep helping refreshing article having no toxic side effects, is essential in the household and indoor health, and is an ideal essential goods for insomniacs.
DE102006047157A1 Cosmetic or dermatological composition comprises 2-isopropyl-5-methylcyclohexylcarbonyl-D-alanine methyl ester and a skin lightener Cosmetic or dermatological composition comprises 2-isopropyl-5-methylcyclohexylcarbonyl-D-alanine methyl ester (I) and a skin lightener. - ACTIVITY : Dermatological. No biological data given. - MECHANISM OF ACTION : None given.
CN101157726A Deuterohemin short-peptide compound and its application in preparation of anti-cataractogenesis drugs The present invention discloses a deuterohemin short peptide compound, including deuterohemin Dh and short peptide Beta-Ala-His-X-Lys, wherein, X can be Thr-Val-Glu or an amino acid sequence with any one amino acid of which being substituted by the corresponding Beta-amino acid and Gamma-amino acid; the connection mode between the deuterohemin and the short peptide is that the carboxyl group on the deuterohemin is connected with the amino group on a peptide chain by an amido bond; the structure can be a monomer, that is, one of two carboxyl groups on the deuterohemin is connected with the peptide chain, and the two monomer forms are the isomers. The present invention further provides the usage of the compound in the preparation of the anti-cataract drugs.
CN103393638A Application of formononetin in preparing medicine for treating breast cancer The invention discloses a novel use of formononetin in pharmacy, and in particular discloses an application of formononetin in preparing a medicine for treating breast cancer. The applicants discover that formononetin can remarkably inhibit cell proliferation of breast cancer for the first time and discover through experiments that formononetin retards cell cycle by way of inactivating IGF1/IGF1R-PI3K/AKT, so that formononetin generates good activity of inhibiting cell proliferation of breast cancer, and can be used as a cell cycle retardant to replace tamoxifen to inhibit cell proliferation of breast cancer so as to prevent and treat breast cancer. In addition, the applicants in experiments further discover that formononetin can be used as the cycle retardant for cancer cells and has specific targeting to normal cells as an agonist, so that formononetin has very high development value and real application value.
CN103550215A Applications of peptides compound in rhizome sparganii The invention discloses applications of a peptides compound in rhizome sparganii in preparing anticoagulant and/or antithrombosis medicaments. The structural formula of the peptides compound is shown in the formula (I). The peptides compound obtained by separating and purifying rhizome sparganii, and applications thereof are provided for the first time, the compound plays a role in prolonging the prothrombin time (PT), activated partial thromboplastin time (APTT) and thrombin time (TT), has good anticoagulation activity, and provides a powerful basis for developing natural antithrombosis medicaments. The formula (I) is as shown in the specification.
US20100286138 Stable forms of N-(2,6-Dimethyl-4-morpholin-4-yl-phenyl)-3,3-dimethyl-butyramide Polymorphic forms of N-(2,6-dimethyl-4-morpholin-4-yl-phenyl)-3,3-dimethyl-butyramide are provided together with a process for the manufacture of said compound.
US20080027097 Pharmaceutical drug candidates and methods for preparation thereof The present invention is directed to methods of preparation of sulfonate derivatized compounds, e.g., 3-amino-1-propanesulfonic acid and 1,3-propanedisulfonic acid disodium salt with increased purity, with reduced potential for toxic by-products, and that are pharmaceutically useful, e.g., for the treatment of amyloidosis.
WO2006077427A3 Antiviral drug combinations There is disclosed a combined preparation comprising a glycosylation modulator and a membrane fusion inhibitor for combined, simultaneous or sequential use in the treatment of infections caused by viruses bearing glycosylated envelope proteins.
WO2012073217A1 Process for the preparation of morpholinyl anthracycline derivatives The present invention provides a process for the preparation of a morpholinyl anthracycline derivative in good yields and purity, including 3'-deamino-3"-4'-anhydro- [2"(S)-methoxy-3"(R)-hydroxy-4"-morpholinyl] doxorubicin (1).
EP2237782A1 Use of tetrahydropyrimidines Tetrahydropyrimidines of the formula in which R is a hydrogen atom or a hydrocarbon radical having up to eight carbon atoms, R’ is hydrogen, OH or OR", and R" is R or COR, where R is defined as above, for use in the prevention or treatment of post-operative inflammatory stress and inflammatory pain.
US20080058332 Antiproliferative, antitumor agents; 4-(3-hydroxyphenyl)-6-morpholino-2-(3-piperidin-4-ylcarbonylaminophenyl)pyrimidine for example The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R1, R2, q, R3, r, R4, X1 and Q1 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.
CN101785771A Compound isoniazid tablet The invention relates to a compound isoniazid tablet used for treating tuberculosis, which comprises isoniazid and vitamin B6, wherein the isoniazid and the vitamin B6 are mixed together and prepared into tablets when preparing the compound isoniazid tablet. Patients with stomach upset for taking the isoniazid can directly take the compound isoniazid tablet to achieve the function of treatment without having any stomach upset, and the invention lays a good foundation for treating the tuberculosis because of being more accepted by patients for reduced total amount of medicines taken.
EP1562615A4 Oral and dental composition The invention provides an oral and dental composition comprising an effective antibacterial amount of a combination of: a) a physiologically acceptable divalent metal ion; b) a quaternary ammonium compound; and c) chitosan or a chitosan derivative in a form to facilitate interaction with the other two components of the combination; and a physiologically acceptable excipient.
CN103462953A Application of Nardoaristolones A in preparation of medicaments for treating tongue cancer The invention discloses application of Nardoaristolones A in preparation of medicaments for treating tongue canner, and belongs to the technical field of new application of the medicaments. In vitro MTT (3-4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anti-tumor activity evaluation discovers that Nardoaristolones A also has a remarkable effect on inhibiting the growth of human tongue cancer cell strains PTca8113 and T6, so that Nardoaristolones A can be used for preparing the medicaments for resisting the tongue caner, and has a good development and application prospect, high inhibiting activity, prominent substantive features and significant progress.
WO2010089355A1 Taurine or taurine-like substances for the prevention and treatment of a disease associated with retinal ganglion cell degeneration The present invention relates to taurine or taurine-like substances for the prevention and treatment of a disease associated with retinal ganglion cell degeneration. More particularly the invention relates to a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis for the prevention and treatment of a disease associated with retinal ganglion cell degeneration.
CN101298452A Preparing methods and uses of S-(-)-nadifloxacin and water soluble salt thereof The invention discloses a preparation method of an S-(-)-Nadifloxacin. 3, 4-difluoro-acetbromanilide is taken as initial material to be synthesized by quinoline, and hydrogenated to directly split out an optical active midbody, then is formed into a ring by oxymethylene, protected by carboxyl, condensed by 4-hydroxy piperidine and finally deprotected and hydrolyzed; the S-(-)-Nadifloxacin is used for reacting with the alkali allowed in medicine to prepare S-(-)-Nadifloxacin water-soluble salt; compared with the prior arts of synthesizing and splitting the Nadifloxacin, the materials of the invention are cheap and easily obtained; the reaction is mild; the yield of the splitting technique is stable; the optical purity is high; a splitting agent can be circularly used; the preparation method of the invention is suitable for industrialization production; the S-(-)-Nadifloxacin water-soluble salt is used in clinic; the antibiotic activity is greatly improved; the toxic and side effects are reduced; and simultaneously the increasing of the water-solubility even enlarges the application of the medicament forms.
WO2011093501A1 Gpr119 agonist Disclosed is a compound represented by general formula (I) or (II) or a salt thereof, which is a GPR119 agonist. Also disclosed is a therapeutic agent for diabetes, which contains the compound or a salt thereof as an active ingredient. In the formulae, one of T1-4 represents N and the others represent CR4, or all of T1-4 represent CR4; R2, 3 each represents H, a C1-8 alkyl group; A represents (CH2)1-3, a single bond or the like; B represents (CR5)1-3, a single bond or the like; one of U and V represents N, and the other represents CR7; "-" between W and X represents a single bond or a double bond; W represents C or CR8; X and Y each represents a C1-3 alkylene group (which may be substituted by Hal, OH or the like) or the like; Z represents COOR9, COR10, an alkyloxadiazolyl group, an alkylpyrimidyl group or the like; Q represents N or CH; A0 represents O, a single bond or the like; B0 represents (CR25)1-3, a single bond or the like; one of U0 and V0 represents N, and the other represents CR27; "-" between W0 and X0 represents a single bond or a double bond; W0 represents C or CR28; X0 and Y0 each represents a C1-3 alkylene group (which may be substituted by Hal, OH or the like) or the like; Z0 represents COOR29, COR30, an alkyloxadiazolyl group, an alkylpyrimidyl group or the like; R1, 7, 8, 20, 27, 28 each represents H, Hal, OH, a C1-8 alkyl group or the like; R5, 25 each represents H, a C1-8 alkyl group or a C3-6 cycloalkyl group; R4, 5, 21-23 each represents H, a C1-8 alkylsulfonyl group, a tetrazolyl group, a triazolyl group or the like; and R9, 10, 29, 30 each represents a C1-8 alkyl group or the like.
CN101209349B Application of carbon nano-tube as carrier in transferring anti-cancer medicine The invention relates to the application of carbon nanotubes in the transport of anti-cancer drugs as carriers. The synthesized carbon oxide nanotubes of the invention can be bonded with different anti-cancer drugs, the drug molecules after the bonding can penetrate the cell membranes to be distributed in the cells and not be discharged. The experimental results show that the drug molecules without bonding carbon nanotubes have great distribution difference in the multi-drug resistance cell system and the mother cell system, the distribution difference after the bonding is reduced significantly, which indicates that the high-expression permeable glycoproteins on the multi-drug resistance cell system can not pump a great number of drug molecules which are bonded on the carbon nanotubes to the outside of the cells, the carbon nanotubes can effectively inhibit the discharging function of the permeable glycoproteins, thereby proving that the carbon nanotubes can be used as the carriers and applied in the transport of the anti-cancer drugs and providing a new thinking for the development of novel anti-cancer drugs, at the same time, the invention can promote the studies of the nano-materials on the drug transport and the aspect of multi-drug resistance mechanism.
US7202085 Acylated Homoserine Lactone (AHL) compounds and AHL receptors derived from bacterial quorum sensing systems; inducible or repressible promotors regulate gene expression in plants and plant cells DNA constructs and other compositions and methods for controlling gene expression in eukaryotic cells and organisms are derived from bacterial quorum sensing systems. One or more cis elements from the luxI promoter (“lux box”) or a functionally similar sequence are incorporated in a eukaryotic promoter. A receptor protein from the LuxR family of transcriptional regulators, upon binding an acylated homoserine lactone (AHL) compound, interacts with the lux box, modulating the activity of the promoter.
WO2013081565A1 Pharmaceutical compositions comprising roflumilast and terbutaline The present invention relates to combined use of roflumilast, which is a selective phosphodiesterase-4 (PDE-4) enzyme inhibitor, and terbutaline, which is a β2adrenergic receptor agonist; and to drug compositions comprising this pharmaceutical combination that can be used in the allergic and inflammatory diseases of skin or upper and lower respiratory tracts.
WO2013182578A1 Use of vitamin k to decrease allograft failure and patient mortality after organ transplantation Poor vitamin K status is provided as an independent risk factor for allograft failure and mortality in patients who received organ transplantation and who are under immunosuppressive medication. Various forms and recommended dosagesof vitamin K, optionally combined with vitamin D and/or other immunosuppressive medication, are provided to optimize the treatment of such patients resulting in decreased allograft failure and improved patient survival.
CN103755687A Hydrochloric tandospirone crystal form I and preparation method of crystal form I The invention provides a hydrochloric tandospirone crystal form I. The hydrochloric tandospirone crystal form I is characterized in that an X-ray powder diffraction pattern of the crystal form I shows that characteristic absorption peaks appear at 2 theta diffraction angles of 6.597+/-0.2, 10.352+/-0.2, 12.676+/-0.2, 15.362+/-0.2, 15.922+/-0.2, 17.122+/-0.2, 18.752+/-0.2, and 25.522+/-0.2 degrees. The invention also provides a preparation method of the crystal form I. Compared with the existing hydrochloric tandospirone product, the hydrochloric tandospirone crystal form I, provided by the invention, has the advantages that the water solubility and the stability are improved, and the bioavailability and the safety of a drug can be improved; in addition, the crystal form is simple in preparation process, high in yield, and suitable for industrial production.
EP1818328A1 Chromatographic method for the isolation and purification of taxane derivatives A method is disclosed for obtaining an organic solution of paclitaxel by way of novel purification technology. The method uses a "Load and Lock Axial Compression Column" for industrial scale preparative high performance liquid chromatography. The "Load and Lock Axial Compression Column" is one in which a piston is used to pack and unpack the chromatography bed substantially to avoid voids therein, and to maintain bed compression during use. This maintenance of the compression effectively and substantially prevents the formation of voids in the bed, which increases the efficiency of the procedure. The column can be packed with any packing material, including small particle size (e.g., about 10 µm) media. In this way, very high plate numbers are generated. The bed length can be adjusted by controlling the amount of packing material used to prepare the column. Additional steps enable paclitaxel to be isolated with a purity of 99% or more, and for crystalline 9-dihydro-1,3-acetylbaccatin III to be isolated for use in medicaments.
WO2009011880A3 Heterocyclic modulators of pkb The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
WO2005079778A3 Medicaments for treating barrett’s oesophagus The present invention relates to the use of a retinoic acid antagonist in the manufacture of a medicament for the treatment or prevention of Barrett's oesophagus (Barrett’s mucosa). Furthermore, the invention relates to use of a retinoic acid antagonist in the manufacture of a medicament for the treatment or prevention of ectopic development of columnar epithelium, use of such an antagonist in the conversion of columnar epithelium to squamous epithelium, in the induction or maintenance of squamous epithelium, and in the reduction of proliferation. of ectopic columnar epithelium. Preferably the retinoic acid antagonist is an aldehyde dehydrogenase inhibitor such as a competitive inhibitor. Preferably the antagonist is citral.
CN102512358A Rifaximin vaginal suppository for livestock and preparation method for same The invention belongs to the field of veterinary medicine, and particularly relates to a rifaximin vaginal suppository for livestock and a preparation method for the same. The suppository contains the following components: 8.5-25.5 parts by weight of rifaximin solid dispersion, 30-88 parts by weight of matrix, 6.0-12.5 parts by weight of water, 0.01-1.0 parts by weight of surfactant, 0.01-10.0 parts by weight of synergist and 0.01-5.0 parts by weight of preservative, wherein the rifaximin solid dispersion is obtained by melting 7.3-21.9 parts by weight of solid dispersion carrier in a water bath at 70-80 DEG C, and then adding the used 2-16 parts by weight of absolute ethyl alcohol to dissolve 1.2-3.6 parts by weight of rifaximin to obtain rifaximin solution, uniformly stirring, steaming away the absolute ethyl alcohol in the water bath at 70-80 DEG C, and then rapidly cooling and solidifying. The suppository disclosed by the invention can ensure the uniform dispersion of main medicine and overcome the problems of low heat resistance and long melting time limit of glycerin gelatine matrix.
WO2008102912A1 Target protein and target gene for drug discovery, and screening method Disclosed are: a target protein and a target gene for a physiologically active substance such as a drug; and a means for developing a novel physiologically active substance by using the target protein or the target gene. Specifically disclosed are: a target protein and a target gene for a physiologically active substance; a method for the screening of a substance capable of regulating a physiological activity; a regulator of a physiological activity; a method for producing a derivative of a physiologically active substance; a complex comprising a physiologically active substance and a target protein, and a method for producing the complex; a kit comprising a physiologically active substance or a salt thereof; a method for the determination of the occurrence or the risk of occurrence of a given disease or condition; a method for the determination of the sensitivity to a physiologically active substance and a determination kit for use in the method; and others.
CA2184828C Composition for inactivating irritants in fluids A composition of matter for applying to a surface which comprises an irritant-inactivating agent, and a substance which substantially prevents the irritant-inactivating agent from binding to the surface, wherein the irritant-inactivating agent in the composition is present in an amount effective to inactivate irritants in fluids which contact the composition is described. Surgical instruments and physical barriers with the aforementioned composition applied thereto are also described. A method of inactivating irritants in a fluid contacting skin comprising applying the aforementioned composition to the skin is also disclosed. A method of inactivating irritants in a fluid contacting skin covered with a physical barrier comprising applying the aforementioned composition to the skin is also disclosed.
US7214715 Substituted hydroxyl amine derivatives; inhibitors of beta-secretase, inhibit beta-secretase-mediated cleavage, inhibitors of A beta production, and/or are effective to reduce amyloid beta deposits or plaques The present invention is substituted amines of formula (X) and of the formula (X′) useful in treating Alzheimer's disease and other similar diseases.
WO2008046087A2 Spiro compounds and their uses as therapeutic agents This invention is directed to spiro-benzoisothiazole derivatives of formula (I), wherein j, k, m, q, Z, Q, R1, R2 and R3 are each as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
US20060223839 5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-5H-chromeno-[3,4-f]-quinolines as selective progesterone receptor modulator compounds The present invention is directed to compounds, pharmaceutical compositions and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such compounds and pharmaceutical compositions.
CN103396521A Synthesis and micellization application of amphiphilic beta-cyclodextrin star polymer The invention belongs to the technical field of high polymer chemistry and pharmaceutical preparations, relates to a synthesis and a micellization application of an amphiphilic beta-cyclodextrin (beta-CD) star polymer, and provides an amphiphilic beta-cyclodextrin (beta-CD) star polymer taking beta-cyclodextrin (beta-CD) as a core, acrylic acid and a methyl methacrylate copolymer as a lipotropy block and poly (N-vinyl pyrrolidone) as a hydrophilic block, and a synthesizing method of the amphiphilic beta-cyclodextrin (beta-CD) star polymer. The amphiphilic beta-cyclodextrin (beta-CD) star polymer is formed by connecting amphiphilic block polymers to 3-6 hydroxide radicals of the beta-cyclodextrin (beta-CD). The molar mass ratio of the acrylic acid and the methyl methacrylate in the lipotropy block and the poly (N-vinyl pyrrolidone) in the hydrophilic block in the amphiphilic polymer is 4:1:(1-15):1:16. The invention further relates to a vinpocetine micelle taking the amphiphilic beta-cyclodextrin (beta-CD) star polymer as a carrier material and a preparation method of the vinpocetine micelle. The medicine carrying micelle of the amphiphilic beta-cyclodextrin (beta-CD) star polymer provided by the invention has the characteristics of slow-release effect, pH sensitivity and lung targeting.
CN101810581B Method for enhancing content uniformity of clenbuterol hydrochloride and application thereof The invention relates to a technological measure for enhancing the content uniformity of clenbuterol hydrochloride and application thereof. A technological method comprises the following steps: dissolving the clenbuterol hydrochloride and a pharmacologically-acceptable carrier in a solvent to prepare solution or suspension; and drying the solution or the suspension to form dry particles or powder.
CN101371142A Method of diagnosis and method of treatment The present invention relates to a method for diagnosing higher susceptibility for diseases and conditions associated with low levels of AKG in a human or animal comprising the following steps: a) obtaining a biological sample from said human or animal; b) measuring the alpha-ketoglutaric acid (AKG) level in the biological sample; and c) comparing said measured AKG level with normal average AKG levels, wherein a level of AKG in said sample lower than an average level is indicative of a higher susceptibility for various diseases. Further the invention relates to a use of a substance comprising at least one member selected from the group consisting of AKG and derivates, metabolites, analogues or salts thereof for the manufacture of a pharmaceutical preparation or a food or feed supplement for the treatment or prophylaxis of diseases and conditions associated with low levels of AKG in a human or animal with low levels of AKG compared with normal average AKG levels.
CA2447878C 5-chloro-3-(4-methanesulfonylphenyl)-6'-methyl-[2,3']bipyridinyl in pure crystalline form and process for synthesis This invention encompasses a pharmaceutical composition comprising the compound of formula A: A in combination with a pharmaceutically acceptable carrier, said compound being comprised of about 1-50%, 1-20% or 1-10% of the polymorphic form which is designated Form V and the remainder of the compound being comprised of at least one polymorphic form selected from the group consisting of: Form I, Form II, Form III and Form IV
CN102000148B Application of scutelaria baicalemis and baicalin in preparing medicament for improving learning memory and treating Alzheimer's disease The invention discloses novel application of scutelaria baicalemis and baicalin in preparing a medicament for improving learning memory and treating Alzheimer's disease. In the application, the scutelaria baicalemis and the baicalin can improve the learning memory capability of a naturally rapidly aged mouse and a rat suffered from Alzheimer's disease (AD), and can treat AD by inhibiting beta toxicity of amyloid peptide section and other aspects; the baicalin can remarkably improve the sugar metabolism level of the model rat suffered from AD in treating the AD, and can improve the learning memory capability of the rat suffered from AD; neurotransmitter detecting experiments discover that the baicalin can improve the contents of norepinephrine, dopamine and serotonin in cerebral cortex of the rapidly aged mice.
US7045594 Serine proteinase inhibitors A serine protease inhibitor, characterized by having a domain with four cysteines, and a sequence of 0 to 20 amino acids is present between the first and second cysteines, or the serine protease inhibitor has a domain with six cysteines, and a sequence of 7 to 20 amino acids is present between the first and second cysteines.
US7402688 novel 2,2-disubstituted-19-norvitamin D derivatives and 20-epi-19-norvitamin D derivatives; metabolic regulatory hormone of calcium and phosphorus; biological activities: cellular induced differentiation, suppression of proliferation, and immunomodulation by transcription control of target gene A novel 2,2-di-substituted 19-norvitamin D derivative. It is a compound represented by the general formula (I) wherein R1 and R2 are the same or different and each represents hydroxy and A represents hydrogen, or an unsubstituted linear or branched alkyl.
US20090156654 Derivative n-thiolated 2-oxazolidinone antibiotics This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylococcus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.
US8778962 Treatment of solid tumors with rapamycin derivatives Rapamycin derivatives have interesting effects in the treatment of solid tumours, optionally in combination with a chemotherapeutic agent.
EP2288352A2 Clonidine formulation in a polyorthoester carrier Effective treatments of acute pain for extended periods of time are provided. The treatments include the administration of one or more drug depots at or near a target site wherein the drug depots include an effective amount of clonidine formulated within a polyorthoester. By administration of one or more drug depots at or near the target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days or at least one hundred and thirty-five days.
EP2439197A1 Substituted benzimidazole derivatives as melanocortin 4 receptor antagonists The present invention relates to substituted benzimidazole derivatives as melanocortin-4 receptor (MC-4R) modulators.
CN103156699A Vagina embolism device of cow synchronization of estrus and preparation method thereof Provided is a vagina embolism device of cow synchronization of estrus. The vagina embolism device of cow synchronization of estrus is in a Y shape and is composed of a plastic skeleton, silicon rubber medicine slow release caps and a plastic digging rope. Two cylinder slice layer shape silicon rubber medicine slow release caps are sleeved on two upper forks of the Y-shaped plastic skeleton. The cylinder slice layer shape silicon rubber medicine slow release caps are prepared by mixing vinyl silicon rubber, silicon rubber cross-linking agent, flugestone powder and stearic acid slow-release formulation according to a ratio and through ejection molding. When the vagina embolism device of cow synchronization of estrus is used, all parts are assembled and placed in the vagina of a cowinestrus and taken out in 10 to 15 days. Flugestone hormone is utilized to inhibit natural estrus action of the cow, when the action is relieved, the cow group can rut synchronously, and a goal of controlling animal estrus through manual work can be achieved.
US7666873 N-phenyl-(2R,5S)dimethylpiperazine derivative The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.
CN1927311A Drug for treating chronic atrophic gastritis precancerous lesion and finished capsule product thereof The invention relates to a medicine for treating the lesion of chronic atrophic gastritis, which can replace stomach acid, neutralize stomach alkali, and resist cancer. Wherein, the invention is characterized in that: first using food organic acid as citrate (citrate) to replace stomach acid, neutralize stomach alkali, resist cancer, and prevent cancer, and using its oxidation resistance function to treat chronic atrophic gastritis. And the invention mixes the extractives with SOD activity and cancer resistance function with the acid alkali resistant drug, to treat cancer. Wherein, it comprises B group vitamin to be mixed with acid compounds. The invention can baffle the plantation of gastric cancer cell and avoid the transition of original position.
US20090076079 Deuterium-enriched methylphenidate The present application describes deuterium-enriched methylphenidate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN101906029A Flavonoid derivative , preparation method thereof and use thereof The invention relates to polyphenols substances, a synthesis method thereof and the use thereof, in particular to a flavonoid derivative, a preparation method thereof and the use thereof, and solves the problem that the conventional natural flavonoids compounds are difficult to extract and obtain and cannot be widely used. The structural formula (I) of an intermediate and the structural formula (II) of a final product are shown below, wherein R1, R2 and R3 are respectively selected from hydrogen, C1-C8 alkyl, halogen, nitro, C1-C8 alkoxy and amino; and R1, R2 and/or R3 can be fused with a benzene ring to form a substituted or unsubstituted fused ring compound; R4 and R5 are respectively selected from C1-C8 alkyl, C1-C8 alkoxy and alkylene; R may be H, methoxy-methoxy or methoxy; and b ring is a benzene ring or a heterocyclic compound. The derivative can be used for preparing medicaments for resisting tumors and cardiovascular and cerebrovascular diseases and inhibitors of protein tyrosine kinases, opens up a new way for preparing the medicaments and brings a new breakthrough to the medicament field; and the synthesis method has the advantages of mild condition and convenient operation.
CN1995011A Levo- carnitine calcium fumarate and its preparation method and use thereof The invention discloses a left-handed carnitine calcium fumarate and making method and application, which comprises the following steps: dissolving inner salt of left-handed carnitine in the alcohol or carbinol; adding fumaric acid and alkali with calcium; heating to 70-80 deg. c; stirring sharply; refluxing 1-5h; cooling to -5-5 deg. c to freeze at least 2h; sucking the obtain left-handed carnitine calcium fumarate; drying; obtaining the product; using the composition of left-handed carnitine calcium fumarate to make one or more medical acceptable vehicle and adjunct to supplement calcium.
US20120213866 Method and system for modulating substances affecting bodily processes A method for establishing a treatment for promoting the formation of substances in an individual. The measured or assessed level of substances in the body are compared in order to determine the treatment to provide to an individual.
CA2690877A1 Preventing canker sores The invention relates to preventing the development of a canker sore in the mouth of a person by administering an anti-viral drug to the person before the canker sore develops in the mouth. The invention further relates to packaging the drug as a product for the prevention of canker sores. Valaciclovir is one drug that may be used to practice the invention.
US6919370 Pharmaceutical formulations comprising paclitaxel, derivatives, and pharmaceutically acceptable salts thereof The invention concerns paclitaxel solubilizers and formulations thereof with a high propensity to dissolve paclitaxel. The formulations of the invention reduce or obviate the need for the disadvantageous excipient Cremophor® EL. The formulations of the invention are useful for administering paclitaxel, its derivatives, or pharmaceutically acceptable salts or such derivatives to patients in need thereof. The formulations of the invention are suitable for parenteral, oral, local, or transdermal administration to mammals including humans, particularly for intravenous delivery.
CN1895602A Externally-applied female effervescent tablet for preventing and treating gynecological disease An exterior-applied medicine in the form of effervescent tablet for treating gynopathy is prepared from PP powder, chlorhexidine acetate, citric acid, sodium bicarbonate, menthol, and 7 Chinese-medicinal materials including flaverscent sophora root, cnidium fruit, stemona root, etc.
EP1242411B1 Indole derivatives for the treatment of depression and anxiety The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
US6964954 Use of DHEA derivatives on keratinous substances Methods of improving the appearance of keratinous substances using at least one DHEA derivative such as the skin, hair, eyelashes and/or nails, in particular for preventing or treating cutaneous signs of ageing and/or a faded complexion and/or disorders of pigmentation of the skin or hair and/or drying of the skin and/or hyperseborrhoea and/or imperfections relating to hyperseborrhoea and/or sensitive skin and/or dandruff and/or hair loss and/or canities.
US6919354 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor
US20120095088 Medicinal cannabis uniform in food The invention is a product and a process wherein cannabinoids such as Medicinal Δ9-THC and/or other substances associated with medicinal cannabis, including yet not necessarily limited to cannbidiols, cannabigerol are contained or processed into foodstuffs or medicinal compounds in controlled ways and with specific characteristics. First a medicinal substance with a known about of medicinal cannabis is mixed into a foodstuff such that the medicinal cannabis is distributed uniformly in the foodstuff. Foodstuffs consistent with this invention include baked goods, hard candies, ice cream, bases, ice cream, and yogurt. The product is characterized by a controlled amount of cannabinoids per unit volume of the foodstuff. Another provision of the invention is providing controlled amounts or ratios of Δ9-THC as compared to CBD in a foodstuff.
WO2009015491A1 Umps isoforms as novel predictive markers and therapeutic targets for chemotherapeutics a method of predicting a subject's response to a chemotherapeutic treatment comprising the steps of: obtaining a sample from the subject, detecting a target gene in the sample, and assessing sample to detect at least one isoform of the target gene. if an isoform is detected, then identifying and quantifying isoform. the quantified isoform is compared to a suitable control. a change in expression of the quantified isoform relative to the control indicates the subject's responsiveness to said chemotherapeutic treatment. one embodiment relates to assessing a subject's responsiveness to chemotherapeutic treatments comprising 5-fluorouracil, by detecting, assessing and quantifying selected isoforms of uridine 5'-monophosphate synthase gene. another embodiment relates to assessing a subject's responsiveness to chemotherapeutic treatments comprising 5-fluorouracil, by detecting, assessing and quantifying isoforms a and b, and determining the ratio of expression of isoforms a to b compared to the ratio of expression of a suitable control.
WO2014035140A3 Compounds and compositions for modulating histone methyltransferase activity The invention provides DOT1L inhibitors, and also methods and use of the compounds of the invention, by themselves or in combination with other therapies, for treating a disease, disorder, or condition.
CN100584327C Medication composition in use for treating liver disease A composite medicine for treating hepatism, especially the early phase of liver failure is composed of acetylcysteine or its pharmacologically acceptable salt and at least one medicine for treating hepatism, which is chosen from kurarinol, tiopronin and monoammonium glycyrrhizinate. Its preparing process is also disclosed.
EP1301474B1 Tyrosine derivatives as phosphatase inhibitors Disclosed are compounds of the Formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, R?1, R2, R3, R4 and R5¿ are as defined in the specification. Such compounds are tyrosine phosphatase inhibitors and useful in the treatment or prevention of Type II Diabetes Mellitus. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds, a method for treating or preventing Type II Diabetes Mellitus.
CN103638528A Folic acid targeted nano-particle as well as application and synthesis and detection method thereof The invention relates to a folic acid targeted nano-particle as well as application and a synthesis and detection method thereof. After being administrated, an anti-tumor medicament is in non-specificity arrangement in a body and is large in toxic and side effects and low in therapeutic index. The problem can be effectively solved by adopting a medicament carrier, namely, the nano-particle which is established by using a nano technique and has an active targeting function. Folic acid is an ordinary targeting molecule, the medicament is guided to actively target tumor cells with folic acid receptors, and the anti-tumor effect of the medicament is improved. A novel folic acid targeted nano phytosterol-sodium alginate nano-particle is established by using phytosterol and sodium alginate, a hydrophobic anti-tumor medicament, namely, doxorubicin, is wrapped inside a hydrophobic kernel and is prepared into the nano-particle with the medicament, so that sodium alginate and phytosterol are made into a novel material serving as an anti-tumor medicament carrier, the self-assembled phytosterol-sodium alginate nano-particle as the anti-tumor medicament carrier has the security, effectiveness and targeting capability, and theoretical basis is provided for the nano-particle which is used as a novel medicament carrier in future.
WO2011137528A1 Methods and compounds for inhibiting glycosyltransferases The invention provides, in part, compounds that are capable of inhibiting a glycosyltransferase, such as a uridine diphospho-N-acetylglucosamine:polypeptide β N-acetylglucosaminyltransferase, an alternative N-acetylglucosaminyltransferase, an N-acetylgalactosaminyltransferase, a fucosyltransferase, a xylotransferase or a sialyltransferase. The invention also provides methods for using the compounds.
CN102641252A Terbinafine hydrochloride solid dispersoid and tablet thereof The invention relates to a terbinafine hydrochloride solid dispersoid, which is composed of terbinafine hydrochloride and carrier materials, wherein the proportion by weight between the terbinafine hydrochloride and the carrier materials is 1/2-1/15. The invention further relates to a tablet prepared by the terbinafine hydrochloride solid dispersoid. Compared with the prior art, the terbinafine hydrochloride tablet has the advantages of (1) improving dissolution in vitro of terbinafine hydrochloride preparation; (2) solving the problem that the terbinafine hydrochloride is poor in oral administration absorption and low in biological availability; (3) covering harmful odor and irritation of the terbinafine hydrochloride; (4) keeping pesticide effects of large dose while reducing using quantity of active ingredients in the preparation per unit, and reducing drug side-effects; and (5) being simple in preparation process and suitable for industrial production.
US20080299215 Deuterium-enriched lestaurtinib The present application describes deuterium-enriched lestaurtinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20120141577 Linear expression cassette vaccines The disclosure relates to a linear expression cassette (LEC) as a nucleic acid based vector for producing a gene product of interest. Methods of preparing a disclosed LEC, as well as methods for its use to express a gene product in a subject, are also described. An LEC may be used in an animal or human subject to produce a therapeutic and/or immune response in the subject, such as an immunized state.
EP2328580A1 Dabigatran for percutaneous interventional cardiac catheterisation The invention relates to a new use of dabigatran etexilate of formula (I) optionally in the form of the pharmaceutically acceptable salts thereof, and new medicament formulations which may be used for this purpose.
EP2623490A1 2-(3-aminophenoxy)-acetic acid derivatives as EP2 receptor agonists for use in treatment of glaucoma Aniline derivatives, their preparation and their therapeutic application as EP2 agonists in, for example, glaucoma. R1 represents, independently from each other, H, a (C1-C6) alkyl or an halogen, R2 represents H, an halogen, or a (C1-C6) alkyl, R3 represents, independently from each other, H, an halogen, -OH, -O-(C1-C6) alkyl or a -(C1-C6) alkyl.
EP1326596B1 Pharmaceutical preparations containing a dibenzocyclooctane lignan derivative for prevention and treatment of neurodegenerative disease The invention relates to pharmaceutical preparations containing a dibenzocyclooctane lignan derivative for prevention and treatment of neurodegenerative disease.
CN1732968A Vaginal applied cream with clindamycin and metronidazole and method for preparing the same The invention relates to vagina cream of clindamycinum and metronidazole and its preparing process, which uses the salts or esters of clindamycinum and metronidazole as the active constituents.
CN102429901A Application of indole-3-carbinol, diindolylmethane and derivatives thereof in preparation of medicaments for preventing and treating renal fibrosis The invention provides new application of indole-3-carbinol, diindolylmethane and derivatives thereof in preparation of medicaments for preventing and treating renal fibrosis. The indole-3-carbinol (I3C), diindolylmethane (DIM) and derivatives thereof can be used for preventing and treating the renal fibrosis by inhibiting the activation of renal fibroblasts. The DIM, the I3C and the derivatives thereof can effectively reduce the pathogenetic symptoms of a renal fibrosis animal model, and can become candidate medicament molecules for preventing and treating the renal fibrosis. Meanwhile, the small molecular medicaments are easily obtained, have low price and stable properties, are convenient to preserve and transport, and have broad application prospects.
US20110124644 Methods of diagnosing and characterizing cannabinoid signaling in crohn's disease Diagnosis of Crohn's Disease by determining the presence or absence of variants at the CNR2 (cannabinoid) genetic locus and serological markers is disclosed Methods of diagnosing a Crohn's Disease sub-type by determining the presence or absence of one or more risk variants at the CNR2 5 locus and the presence or absence of ASCA, OmpC, 12 and/or anti-Cbir1 antibodies are included
US20130281704 Salts of benzimidazole compound and use thereof A sodium salt, magnesium salt, lithium salt, potassium salt, calcium salt or barium salt of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole, and a pharmaceutical composition comprising the salt. The novel salt is useful as an excellent antiulcer agent.
CN103127134A Medicine composition containing fluticasone propionate and nitric oxide synthase (NOS) inhibitor and for treating nose inflammation A medicine composition containing fluticasone propionate and a nitric oxide synthase (NOS) inhibitor and for treating nose inflammation comprises the fluticasone propionate serving as an active constituent, an amino acid derivative serving as the NOS inhibitor, one or more types of medicine auxiliary materials suitable for nose medicine dosing and the balance water.
US20100256155 Method for inhibiting growth of cancer cells and cell telomere and diseases of cell proliferation by using heteroannelated anthraquinone derivative compounds A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of i) a first substituent being one selected from a group consisting of a hydryl group, an amino group, a nitro group, a hydroxyl group and a cyan group, ii) a second substituent being one selected from a group consisting of (CH2)nX, a straight (CH2)n alkyl group, a (CH2)n alkoxyl group, a branched (CH2)n alkyl group, a C3˜C12 nephthenic group, and a C3˜C12 cyclic alkoxyl group, wherein 1≦n≦12, and X is a halogen, iii) a third substituent being one selected from a group consisting of a straight C1˜C8 alkyl group with a double-bond, a C1˜C8 alkoxyl group with a double-bond, a branched C1˜C8 alkyl group with a double-bond and a C3˜C8 nephthenic group with a double-bond, and iv) a fourth substituent of a C5˜C12 heterocyclic group.
EP2643321A1 Imidazo [1,2-b]pyridazine and imidazo [4,5-b]pyridine derivatives as jak inhibitors New imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
WO2013061919A1 Novel compound and method for producing same The purpose of the present invention is to provide: a novel compound useful as an anti-mold substance; and a method for producing the compound. The present invention relates to: a compound represented by formula (I0) (wherein R1 represents a group represented by formula (2); and R2 represents a group represented by formula (3) or a salt thereof; and a method for producing the compound using a microorganism.
CN102670516A Tilmicosin soluble powder and preparation method thereof The invention discloses tilmicosin soluble powder, which consists of the following components in parts by weight: 1-50 parts of tilmicosin, 1-50 parts of a solid dispersoid carrier auxiliary material and 0-70 parts of a medical filling auxiliary material. The invention further discloses a preparation method of the tilmicosin soluble powder. The method comprises the following steps of: (1) adding the solid dispersoid carrier auxiliary material into a solubilizing assistant for dissolving; (2) adding tilmicosin, stirring and dissolving; and (3) drying. The tilmicosin soluble powder disclosed by the invention has the advantages of low water content, high solubility, high bioavailability and convenience for administration, and the palatability of animals can be improved simultaneously.
US20080159977 Modified, protease resistant, colony stimulating factor for use in treatment and prevention of autoimmune and cell proliferative diseases; directed protein evolution Compositions of modified cytokines and uses thereof generated using processes and systems for the high throughput directed evolution of peptides and proteins, particularly cytokines that act in complex biological settings, are provided. Also provided are modified cytokines formulated for oral delivery and uses thereof to treat diseases and conditions mediated by cytokines.
WO2008037182A1 Use of ginsenoside rg1 for treatment of cerebral ischemia and/or diseases or symptoms induced by cerebral ischemia Use of ginsenoside Rg1 for prevention, alleviation and/or treatment of cerebral ischemia and/or diseases or symptoms induced by cerebral ischemia. Use of ginsenoside Rg1 in preparation of pharmaceutical compositions for prevention, alleviation and/or treatment of cerebral ischemia and/or diseases or symptoms induced by cerebral ischemia. Method of prevention, alleviation and/or treatment of cerebral ischemia and/or diseases or symptoms induced by cerebral ischemia, comprising administration a treatment effective amount of ginsenoside Rg1 containing pharmaceutical compositions to the subjects in need thereof.
CN101638652B RNA interfering target of osteoclast V-ATP enzyme proton pump sub-unit ATP6vlcl and application thereof The invention belongs to the technical field of molecule biology and biomedical science, and relates to targets in a C1 sequence for RNA interference, SiRNA obtained in various ways for the targets and application thereof in preparing new medicines for treating osteoporosis. A slow virus is used for infecting osteoclast and expressing ShRNA, and a method of osteoclast function detection after in vitro gene is knocked down is also used; thus, targets for RNA interference in C1 genes are screened. ShRNA for the targets can obviously inhibit the expression of C1 protein, stably inhibit the capabilities of extracellular acidification and bone resorption of the osteoclast, and does not affect the formation of filiform actin rings of the mature osteoclast. Based the target sequence, biological medicines for treating osteoporosis can be prepared.
CN101134724A 1'-acetoxy chavicol acetate The present invention relates to process of producing intermediate product p-hydroxy phenyl propenyl-1-alcohol through reaction of the materials magnesium vinylbromide and p-hydroxy benzaldehyde and the subsequent acetylation reaction to synthesize 1'-acetoxy chavicol acetate, and the application of 1'-acetoxy chavicol acetate in medicine, food and daily chemical product.
WO2009113404A1 Inhibitor for growth of bacteria of genus legionella, bath agent and cleaning agent An inhibitor for growth of bacteria of the genus Legionella contains, as an active ingredient, an extract of Macaranga tanarium extracted from Macaranga tanarium using an extraction solvent containing at least an organic solvent. Alternatively, the inhibitor for growth of bacteria of the genus Legionella contains, as an active ingredient, at least one member selected from NYMPHEOL-A, NYMPHEOL-B and NYMPHEOL-C. The inhibitor for growth of bacteria of the genus Legionella is used, for example, by adding it to a bath agent and a cleaning agent.
EP2561767A1 Epicatechin for alleviating symptoms of allergy The present invention relates to epicatechin for use in the prevention or reduction of symptoms of an allergic disorder and/or an allergic reaction. The invention further relates to epicatechin for said use in the form of food, food product, food supplement or pharmaceutical products.
WO2005113515A8 Pyrimidines for use as plk inhibitors The invention relates to the compounds of formula (1), wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2 and R3 are defined as in claim 1. These compounds are suitable for use in the treatment of diseases which are characterized by excessive or abnormal cell proliferation. The invention also relates to the use of these compounds in the production of a drug having the above-mentioned properties.
US20100226960 Natural biodegradable matrices and uses thereof Matrices formed from a natural biodegradable material and that exhibit surface degradation in the presence of an enzyme are described. Matrices including a bioactive agent can be implanted or formed in a subject for release of the bioactive agent upon degradation of the matrix. The matrix can be provided in various forms, including coatings for implantable devices, implants, and in-situ formed matrices. The matrix can also be in the form of a medical device having a structure that is used to treat a medical condition.
US20080003284 Levothyroxine compositions and methos The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as levothyroxine (T4) sodium and liothyronine (T3) sodium (thyroid hormone drugs), preferably in an immediate release solid dosage form. Also provided are methods for making and using such immediate release and stabilized compositions.
WO2009007457A2 Compounds and methods for modulating rho gtpases The present invention relates to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac GTPases (Rac1, Rac1b, Rac2 and/or Rac3).
WO2013178856A1 Composition for use as an antifungal agent The invention relates to a composition comprising chitosan, or a chitosan oligosaccharide, and an inhibitor of the ARL1 gene or fluconazole, which can be used to inhibit growth in eukaryotic cells. The invention also relates to the use of the composition as an antifungal agent and for the prevention and/or treatment of fungal infections.
CN102335437A Application of metadherin (MTDH) gene vaccine in preparation of breast cancer cell growth inhibitor The invention belongs to the field of biotechnologies, and relates to a gene vaccine capable of inhibiting cancer cell growth. The gene vaccine can express a cell membrane surface protein metadherin (MTDH) and thus being named as a MTDH gene vaccine. The MTDH gene vaccine is utilized for immunization in an oral way. The MTDH gene vaccine can activate an immune response of CD8+ cytotoxic T cells on breast cancer cells 4T1 expressing MTDH antigens. The MTDH gene vaccine can inhibit breast cancer cell growth and pulmonary metastasis. Through being combined with adriamycin, the MTDH gene vaccine can improve adriamycin effects of inhibiting breast cancer cell growth and pulmonary metastasis, and prolong a life of a mouse loaded with cancer. More significantly, the MTDH gene vaccine does not produce obvious damages on main organs of a human body. Therefore, the MTDH gene vaccine provides a novel approach for improvement of the existing breast cancer treatment method.
US20080033040 Methods And Compositions For Screening Involving Endothelial Cells Under Shearing Conditions The present invention concerns screening methods and compositions relating to endothelial cell function. More specifically, it provides screening methods to identify or characterize pathways and factors involved in endothelial cell function by employing conditions that simulate physiological stress. Additional methods can be implemented to identify candidate drugs for the treatment of endothelial cell dysfunction, such as cardiovascular disease or diabetes.
WO2011109367A3 Methods and compositions for treating or preventing symptoms of hormonal variations The present invention relates to methods, compositions, and kits for treating or preventing symptoms of hormonal variation. The method comprises the steps of administering an effective amount of a receptor antagonist to a subject having one or more symptoms of hormonal variations. The receptor antagonist binds to at least one receptor selected from a serotonin type 2A (5-HT.sub.2A) and/or a dopamine type 2 (D.sub.2) receptors.
US20130035306 Process for preparing purine nucleosides The present invention provides for the preparation β-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and solvent. The present invention also provides for the stereoselective preparation of 2-deoxy-β-D-adenine nucleosides wherein a blocked 2-deoxy-α-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative. The forgoing aspects of the present invention are utilized in the preparation of a clofarabine composition wherein the ratio of β to α-anomer is at least 99:1.
EP1781274A1 Novel biaromatic compounds which activate receptors of ppar type and their use in cosmetic or pharmaceutical compositions The invention relates to novel biaromatic compounds which correspond to the following general formula (I) and to their method of preparation and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology and in the field of cardiovascular diseases, of immune diseases and/or of diseases related to the metabolism of lipids) or alternatively in cosmetic compositions.
WO2013169907A1 Alpha 7 nicotinic acetylcholine allosteric modulators, their derivatives and uses thereof The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
WO2009114089A3 Using fullerenes to enhance and stimulate hair growth Described herein are methods for treating lack of hair growth or a reduction or loss of existing hair by stimulating and/or restoring hair growth, or preventing hair loss. The methods comprise administering to a subject in need thereof a therapeutically effective amount of a fullerene.
CN102049035A Starch polysaccharide-iron compound preparation The invention discloses a starch polysaccharide-iron compound preparation. The starch polysaccharide-iron compound preparation is characterized in that the starch polysaccharide-iron compound preparation is prepared by combining starch polysaccharide-iron, calcium carbonate, casein phosphopeptides and vitamin C together according to a certain proportion. The starch polysaccharide-iron compound preparation has the advantages of reasonable composition and high absorption ratio of iron and calcium, has the effects of treating the iron-deficiency anemia and supplementing calcium, and is particularly applicable to pregnant women, children, old people and other crowds tending to suffer from iron-deficiency anemia and calcium deficiency.
WO2006042728A2 Use of stable ammonium liponate salts for the treatment of diabetic and other disorders The invention relates to the use of stable ammonium α-liponate salts for the treatment of a series of disease states, in particular, diabetic disorders and disorders of diabetic origin. The salts (Lp) (A) are formed from a-liponic acid (Lp) and amino compounds (A) of general formula (II) or (III).
CN102125564A Novel application of ginsenoside PT in treating diabetes and metabolic syndrome The invention provides a novel application of ginsenoside PT in treating diabetes and metabolic syndrome. Ginsenoside PT can improve the sensitivity of peripheral tissue to insulin, can further improve insulin resistance, and can be used for treating diabetes and metabolic syndrome. The invention provides the novel clinical application of ginsenoside PT in treating diabetes and metabolic syndrome for the first time, discloses the action of ginsenoside PT in improving insulin resistance in adipose cells and diabetic obesity db/db mouse model, and clearly demonstrates the effect of ginsenoside PT in improving insulin sensitivity.
WO2010049898A1 Injectable polydeoxyribonucleotide composition for the treatment of osteoarticular diseases Composition based on polynucleotides extracted from natural sources for use in therapeutic treatment and/or as a therapeutic co-adjuvant in the treatment of degenerative diseases of the joints, in particular osteoarthritis.
CN101297796A Grifola frondosa beta-dextran freeze-dried powder for injection The invention relates to a freeze-dried powder for injection which is prepared by Beta-glucan that is extracted and separated by using Grifola frondosa mycelium and has the structure shown in the attached figure I and a preparation method thereof, which pertains to the technical field of medical preparations. The figure shows that monosaccharide of the polysaccharide are composed of glucose, the glucose residue of a main chain is connected by a Beta-1, 6-glycosidic bond, the glucose residue of a branched chain is connected by a Beta-1, 3-glycosidic bond, the length of the branched chain is 2 glucose residues, and the degree of branch is about one half. The range of the molecular weight of the Beta-glucan is 50,000 to 250,000 Daltons, and the distribution width of the molecular weight is less than 3.0. The glucan is a single component with a certain range of the molecular weight, and the molecules of the component have the same repeated unit structures regardless of the size of the molecular weight. The tests prove that the freeze-dried powder for injection provided by the invention is characterized by immune regulation, anti-radiation and tumor inhibition.
CN102600210A Compound dextromethorphan hydrobromide syrup and preparation method for same The invention provides a compound dextromethorphan hydrobromide syrup and a preparation method for the same. The compound dextromethorphan hydrobromide syrup is used for eliminating phlegm in cough, and comprises dextromethorphan hydrobromide, guaifenesin and a bacillus natto extract. The syrup improves the safety of medication and is especially suitable for children, reduces bitter taste and the consumption of a flavouring agent, improves the stability, especially the colour of solution and the stability of the colour, and improves the curative effect on the cough caused by cold and bronchitis simultaneously.
CN101293041B Externally used medicament for treating protrusion of lumbar vertebral disc, spinal canal stenosis The invention discloses an externally applied drug for treating lumbar disc herniation and spinal canal stenosis, which takes Chinese angelica, sappan wood, red paeony root, danshen root, earthworm, east asian tree fern rhizome, eucommia bark, hairy antler, membranous milkvetch root, combined spicebush root, amur corktree bark, sanchi, common floweringquince fruit, scorpion, ground beetle, slenderstyle acanthopanax bark and borneol as raw materials. The drug of the invention for treating lumbar disc herniation and spinal canal stenosis has significant effects, no toxicity or side effects and difficult recurrence after the cure, and the total effective rate is 95 percent. The people with skin lesions are forbidden to use the drug.
CN103536603A Wettable sulfamonomethoxine (sodium) powder and preparation method thereof The invention relates to the technical field of veterinary medicine preparation, and particularly relates to wettable sulfamonomethoxine (sodium) powder and a preparation method thereof. The wettable sulfamonomethoxine (sodium) powder provided by the invention is added with potassium citrate, a suspending agent and a wetting agent on the basis of effective components of the original medicine; by reasonable medicine proportioning, the invention provides the wettable sulfamonomethoxine (sodium) powder which is easy to disperse evenly in water, convenient to absorb by animals, and small in toxic and side effects. Compared with commercially available compound sulfamonomethoxine (sodium) powder, the wettable sulfamonomethoxine (sodium) powder is convenient to use and good in therapeutic effect. The invention also provides the preparation method of the wettable sulfamonomethoxine (sodium) powder, and the preparation method is simple in technology, low in production cost and suitable to industrialized production.
CN101396353A Use of baclofen in withdrawal treatment of opium drug The invention relates to the application of baclofen in the opium drug abstinence treatment and belongs to the technical field of addiction medicine application. According to the characteristic of baclofen GABA beta-receptor stimulant, the invention applies the baclofen with the daily dosage of 15 to 120mg as the drug for the opium drug abstinence treatment by virtue of the mutual reaction relation between the baclofen GABA beta-receptor stimulant and an opium system, the close relation between a GABA beta-receptor and the opium drug acute abstinence, the advantages of the GABA beta-receptor stimulant reducing the exacting action of the opium drug, etc. The baclofen is concretely applied in the comprehensive treatments, such as opium drug detoxification (acute abstinence symptom), healing (protracted abstinence syndrome and overcoming psychological dependence), etc. The clinical trial shows that the invention not only develops the application range of traditional drugs, but also has the advantages of investment saving, the low cost of product, strong practicability, good effect, etc. The baclofen can be widely applied to the opium drug abstinence detoxification and healing treatment.
WO2013041537A1 Heterocyclocarbonylaminothiazoles, cosmetic or dermatological preparations containing said heterocyclocarbonylaminothiazoles, and use thereof to combat or prevent undesired pigmentation of the skin The invention relates to heterocyclocarbonylaminothiazoles of general formula (I), wherein R 1 = -morpholino, -piperidin-1-yl, -piperazin-1-yl, -((4-alkyl)-piperazin-1-yl), -pyrrolidinyl, -(1H-pyrrol-1-yl), -azetidin-1-yl, -azepan-1-yl, -2,3,4,5-tetrahydro-1-H-azepin-1-yl, -2,3-dihydro-1H-azepin-1-yl, -1H-azepin-1-yl, -tetrahydro-2H-pyran-4-yl, -4H-pyran-4-yl, -2H-pyran-4-yl, -oxepanyl, -dioxanyl, -tetrahydrofuranyl, -pyrrazolyl. The invention further relates to cosmetic or dermatological preparations having an effective content of one or more heteroalkylamidothiazoles and to the use thereof for the cosmetic or dermatological treatment and/or prophylaxis of undesired skin pigmentation.
US20110301133 Compositions of protein receptor tyrosine kinase inhibitors The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
WO2011100282A2 Imatinib mesylate polymorphs The present application relates to crystalline forms of imatinib mesylate and process for preparation thereof.
EP2334681A1 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors Provided are certain 1,2,3,6- tetrahydroazepino[4,5-b]indole-5-carboxylate compounds which are useful for modulating the activity of nuclear receptors, such as farnesoid X receptors, and/or for the treatment, prevention, or amelioration diseases or disorders related to the activity of these receptors.
US20110245287 Hybrid Opioid Compounds and Compositions Disclosed are hybrid opioid compounds, mixed opioid salts, compositions comprising the hybrid opioid compounds and mixed opioid salts, and methods of use thereof. More particularly, in one aspect the hybrid opioid compound includes at least two opioid compounds that are covalently bonded to a linker moiety. In another aspect, the hybrid opioid compound relates to mixed opioid salts comprising at least two different opioid compounds or an opioid compound and a different active agent. Also disclosed are pharmaceutical compositions, as well as to methods of treating pain in humans using the hybrid compounds and mixed opioid salts.
US8716341 Topically applicable compositions for the treatment of keratinization disorders Topical compositions containing from 0.01% to 0.09% by weight of adapalene or salts thereof are useful for the treatment or prevention of keratinization disorders, particularly acne, and additionally contain at least one gelling agent selected from among carbomers, polysaccharides, cellulose and its derivatives, copolymers of acrylate and of alkyl acrylate, copolymers of acrylamide and of sodium acrylamido-2-methylpropanesulfonate, and xanthan gum.
CN103417778A Medicinal liquor for treating beriberi The invention discloses a medicinal liquor for treating beriberi. The medicinal liquor is characterized in that effective components are prepared from the following raw materials by weight: 6-12 g Cantharides, 3-7 g betelnut, 2-8 g scorpion, 6-12 g cicada ecdysis, 5-15 g tender willow leaf and the like. All the medicines are combined to complement one another so as to achieve the effects of counteracting toxic substances, expelling stasis, killing pests, breaking stagnation, detoxifying, and relieving pain, wind-heat and itching. Through the synergistic effect among the medicines, the medicinal liquor has the affects of, heat clearing, diuresis promoting, Yang warming, cold dispelling, detoxifying, pest killing as well as itching and pain relieving, so as to cure the beriberi thoroughly, and prevent the beriberi from relapsing.
CA2547008A1 New class of gamma delta t cells activators and use thereof The present invention relates to a new class of compounds having .gamma..delta. T cells activating properties of Formula (I), a composition comprising these compounds and methods for regulating an immune response in a subject comprising the step of administering these compounds.
CN103313717A Composition containing styraxlignolide A or the aglycone thereof as an active ingredient for preventing or treating asthma The present invention relates to a pharmaceutical composition containing styraxlignolide A or the aglycone thereof as an active ingredient for preventing or treating asthma. More particularly, the styraxlignolide A compound is separated from the stem and bark of Styrax japonica, and the styraxlignolide A or homoegonol, which is the aglycone of styraxlignolide A and which has improved safety, has the effect of attenuating weight loss and hypersensitivity of the airway, inhibiting the generation of active oxygen in the airway, inhibiting the generation of IgE, TGF-beta 1, and IL-17 in the serum and bronchoalveolar lavage fluid, inhibiting inflammatory cell infiltration in the bronchial tubes, and inhibiting the formation of a mucous plug and subepithelial fibrosis in an asthmatic mouse model. Therefore, the above-described styraxlignolide or homoegonol can be effectively used as the active ingredient of a pharmaceutical composition for preventing or treating bronchial asthma in which airway remodeling has progressed.
CN102603856A Anti-tumor saponin in anemone plants and preparation method thereof as well as application The invention relates to a preparation method of a triterpenoid saponin compound in anemone plants and a mechanical application, in particular relates to an anti-tumor application. The molecular formula of the compound is C47H76O16, and a chemical name of the compound is oleanolic acid-3-0-alpha-L-rhamanopyranosyl-(1->2)-[beta-D-glucopyranosyl-(1->4)]-alpha-L-arabinopyranosid. The extraction preparation process of the compound disclosed by the invention is applicable to the industrial production and can be used for converting other saponin compounds in medicinal materials into the saponin through an alkaline hydrolysis production, so that the content of the target saponin compound is greatly improved. Shown by anti-tumor experiments in vivo and vitro, the compound plays a role in suppressing a plurality of kinds of tumor cells to generate, and approximately has no suppression and toxic actions on generation of normal cells. Therefore, the triterpenoid saponin compound can be used for treating tumor diseases.
CN103251608A Application of Myriberine A in preparation of medicines for treating Alzheimer disease The invention discloses a new application of Myriberine A. The Myriberine A has acetylcholine esterase inhibitory activity and a nerve cell protection function; and the Myriberine A can be used for preparing medicines for treating Alzheimer disease as a multipurpose target compound. An application of Myriberine A in preparation of medicines for treating Alzheimer disease is disclosed for the first time, a framework type belongs to a brand-new framework type, the Myriberine A has an unexpected strong effect of inhibiting the acetylcholine esterase activity, and the revelation possibility of other compounds cannot be generated, so the application has obvious substantive features; and moreover, the application has an obvious improved effect of preventing the Alzheimer disease.
EP1140064B1 Oral administration of taxoid derivatives The present invention relates a new pharmaceutical form of taxoid derivatives. It relates more precisely an oral administration of a taxoid bearing two alkoxy groups in position 7 and 10.
CN103720665A Desloratadine citrate disodium composition for injection The invention provides a desloratadine citrate disodium composition for injection. The composition is characterized by comprising desloratadine citrate disodium, mannitol, a pH value modulator and water for injection; the preparation adopts a form of a lyophilized preparation or injection; the composition can remarkably improve medicine stability, and reduce the devitrified phenomenon during a lyophilization process; moreover, the redissolving performance and the safety of clinical medication can be better ensured.
CN101019846A Prepn of capsule containing pyruvic acid and its salt The capsule consists of pyruvic acid and its salt, cane sugar or glucose or fructose, oligose, sodium chloride, potassium chloride, sodium dihydrogen phosphate, vitamin C, vitamin PP, inosite, vitamin B1, vitamin B2, vitamin B5, vitamin B6, vitamin B12 and starch. It has the functions of resisting senility, resisting oxidation, resisting fatigue, preventing cancer, etc. It has convenient taking, good taste, high effect and no toxic side effect.
CN102452990A Homopiperazine acethydrazide derivative with low neurotoxicity and preparation method and application thereof The invention relates to a homopiperazine acethydrazide derivative compound or pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug shown in the formula I, wherein all symbols are described in the description. The invention also relates to the preparation method of the compound, application of the compound in the preparation of drugs for curing and/or preventing tumors and/or cancers, a method for curing and/or preventing tumors and/or cancers by the compound, and a drug compound with the compound with effective quantity for cure and/or prevention. The compound prepared by the invention can selectively kill some cancer cells, and has strong anticancer activity, greatly-reduced neurotoxicity and wide clinic application prospect.
CN101305992A Compound sustained-released injection containing neonatal blood vessel restraining agent The invention relates to a compound sustained-release injection containing neovascularization inhibitors, which comprises sustained-release microspheres and a solvent; wherein, the sustained-release microspheres comprise sustained-release auxiliary materials, neovascularization inhibitors which are selected from Marimastat or fumagillin, etc., and cytotoxic drugs which are selected from hydroxycamptothecine, Mitozolomide, 4-carboxy temozolomide, docetaxel, oxaliplatin, hetaplatin, isophosphamide, lomustine, estramustine, fotemustine, samustine, etoposide, teniposide, catharanthine, anastrozole, fluorouracil, or mitomycin C; the solvent is a special solvent containing a suspending agent. The sustained-release auxiliary materials are selected from decanedioic acid copolymers such as Polifeprosan, polylactic acid, poly (erucic acid dimmer-decanedioic acid) and poly (fumaric acid-decanedioic acid) and so on, EVAc, etc.; the viscosity of the suspending agent ranges from 100cp to 3000cp (when the temperature is 25 to 30 DEG C), and the suspending agent is selected from sodium carboxymethyl cellulose, etc. The sustained-release microspheres can also be made into a sustained-release implanting agent, and can increase the curative effects of the non-operative treatments such as radiotherapy and chemotherapy, etc. when being injected or put in or around tumors.
CN1739520A Sildenafil and its recipe for treating tinnitus and deafness The present invention discloses sidenafil and its compound preparations for treating tinnitus and deafness. The compound preparations include the compound preparation of sidenafil and dihydropyridine as calcium ion antagonist, the compound preparation of sidenafil and ginkgo leaf extract, and compound preparation of sidenafil and red sage and kudzu vine root extracts. The sidenafil and its compound preparations may be prepared into various kinds of orally taken preparation forms, such as tablet, granule, capsule and oral liquid.
WO2009022007A1 Pharmaceutical composition comprising a glucopyranosyl-substituted benzene derivative The invention relates to a pharmaceutical composition according to the claim 1 comprising a glucopyranosyl-substituted benzene derivative in combination with a DPP IV inhibitor which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
US20070232579 Nitrated Lipids and Methods of Making and Using Thereof Described herein are nitrated lipids and methods of making and using the nitrated lipids.
CN102946859A Pharmaceutical compositions of spiro-oxindole compound for topical administration and their use as therapeutic agents This invention is directed to pharmaceutical compositions for topical administration to a mammal, wherein the pharmaceutical compositions comprise a spiro-oxindole compound, as an enantiomer, a racemate or a non-racemic mixture, or a pharmaceutically acceptable salt thereof. These pharmaceutical compositions are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions.
EP0933366B1 5-phenyl-3-pyridazinone derivatives and drug compositions containing the same 5-Phenyl-3-pyridazinone derivatives represented by general formula (I) wherein R1 is optionally substituted C1-C8 alkyl, C3-C7 cycloalkyl, or indanyl; R2 is C1-C4 alkyl; R3 is hydrogen, optionally substituted C1-C5 alkyl, C3-C7 cycloalkyl or aryl optionally containing a hetero atom; R4 and R5 are each independently hydrogen, C1-C6 alkyl, optionally substituted phenyl, or monocyclic aryl containing a hetero atom; and the broken line refers to a single or double bond, with the proviso that when the line refers to the former, R6 is hydrogen or C1-C6 alkyl.
US20060009459 Antidiabetic agents; disease of glucose tolerance; insulin resistance; obesity; dyslipidemia; metabolic disorders; liver disorders Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (Ia): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
US20110212047 Polymer Therapy for the Treatment of Chronic Microvascular Diseases Methods are provided for the treatment of chronic microvascular diseases characterized by inflammation, such as age-related macular degeneration, by administering a polyoxyethylene/polyoxypropylene copolymer. Although a single dose can be effective, multiple treatments can be administered to achieve an optimal and sustained effect. Preferably, a single administration followed by repeated weekly administration of the pharmaceutical composition, but not continuous infusion, achieves a desired effect. Methods of diagnosis and characterization of chronic microvascular diseases using the copolymer are also provided.
EP1425265B1 Derivatives of c2-substituted indan-1-ol systems, methods for the production thereof and their use as medicaments The invention relates to derivatives of C2-substituted indan-1-ol systems and to their physiologically compatible salts and physiologically functional derivatives. The invention concerns compounds of formula (I), wherein the radicals have the cited meanings, their physiologically compatible salts and methods for the production thereof. The compounds are suited for use, for example, as anorectics.
US20110166409 Egfr and pten gene alterations predicts survival in patients with brain tumors The invention relates to methods of predicting the clinical outcome of brain cancer patients based on the LOH levels of the PTEN gene and on the expression levels or the polysomy/amplification levels of EGFR gene in a sample from said patients.
US20080227770 Benzoxazepine Compound A compound represented by the formula [1]: wherein ring A and ring B each represent an optionally substituted benzene ring; ring C represents an optionally further substituted aromatic ring; R1 represents a lower alkyl group optionally substituted with an optionally substituted hydroxyl group; X1a represents a bond or optionally substituted lower alkylene; X1b represents a bond or optionally substituted lower alkylene; x2 represents a bond, —O— or —S—; X3 represents a bond or an optionally substituted divalent hydrocarbon group; Y represents an optionally esterified or amidated carboxyl group, or a salt thereof. The compound of the formula [I] is safer and has more potent lipid lowering activity such as squalene synthase inhibitory activity (cholesterol lowering activity) and triglyceride lowering activity, and thus it is a compound useful as an agent for preventing or treating hyperlipemia.
US20100291191 Tunable sustained release of a sparingly soluble hydrophobic therapeutic agent from a hydrogel matrix The incorporation of polymeric excipients into an injectable hydrogel matrix, for example, methyl cellulose in the case of a hydrogel matrix comprising hyaluronan and methylcellulose (HAMC) has been found to increase the solubility of sparingly soluble hydrophobic drugs and tune their rate of release. The hydrogel matrix may also include other sparingly soluble hydrophobic food or cosmetic agents.
US7365172 Cytoprotective agent to protect a patient undergoing cancer cytotoxic therapy from gastrointestinal side effects; peptide that is derived from a loop or "lollipop" region of transforming growth factor; stimulate hematopoiesis; diabetes, rheumatoid arthritis, lupus, and multiple sclerosis There is disclosed a novel genus of small peptides, much smaller than human TGFα, was discovered as having TGFα biological activity and therefore are useful as pharmacologic agents for the same indications as full length TGFα polypeptide. There is further disclosed that TGFα and consequently the genus of small peptides disclosed herein, was found to have therapeutic activity to stimulate hematopoiesis in patients undergoing cytotoxic cancer chemotherapy and to act as a cytoprotective agent to protect a patient undergoing cancer cytotoxic therapy from gastrointestinal (GI) side effects, such as mucositis and otherwise support the barrier function of the GI tract when it is harmed by cytotoxic therapy.
WO2009060982A1 Cancer cell death inducer having activity of potentiating anti-cancer agent in cancer having resistance against the anti-cancer agent Disclosed is a substance capable of recovering the sensitivity of a cancer cell to an anti-cancer agent and inducing the cell death of the cancer cell in cancer acquiring the resistance to the anti-cancer agent. Specifically disclosed is a cancer cell death inducer for a cancer cell having the resistance against an anti-cancer agent, which comprises DNA for REIC/Dkk-3 as an active ingredient, and which has an activity of potentiating the anti-cancer agent.
US7169769 17α-hydroxy-14β-steroids with hormonal effect This invention relates to steroidal compounds having the formula I wherein: R1 is O, (H,H), (H,OH), NOH, whereby OH is optionally etherified or esterified; R2 and R3 are independently hydrogen or (C1-4) alkyl and at least one of R2 and R3 is (C1-4) alkyl; R4 is hydrogen, or (C1-15) acyl for use in androgen-related treatments, such as androgen insufficiency and male or female contraception.
US20100197645 Thioamide Derivatives as Progesterone Receptor Modulators Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
WO2011130615A3 Preparation of lacosamide Processes for preparing lacosamide, for use in pharmaceutical compositions comprising lacosamide.
US20060025469 Methods for decreasing beta amyloid protein Blood cholesterol levels are correlated with production of amyloid β protein (Aβ), and are predictors of populations at risk of developing AD. Methods for lowering blood cholesterol levels can be used to decrease production of Aβ, thereby decreasing the risk of developing AD. The same methods and compositions can also be used for treating individuals diagnosed with AD. Methods include administration of compounds which increase uptake of cholesterol by the liver, such as the administration of HMG CoA reductase inhibitors, administration of compounds which block endogenous cholesterol production, such as administration of HMG CoA reductase inhibitors, administration of compositions which prevent uptake of dietary cholesterol, and administration of combinations of any of these which are effective to lower blood cholesterol levels. Methods have also been developed to predict populations at risk, based on the role of cholesterol in production of Aβ. For example, individuals with Apo E4 and high cholesterol, defined as a blood cholesterol level of greater than 200 mg/dl, post menopausal women with high cholesterol levels—especially those who are not taking estrogen, or individuals which high blood cholesterol levels who are not obese are all at risk of developing AD if blood cholesterol levels are not decreased.
CN102603826A Method for extracting 8-acetylharpagide from decumbent bugle herb plant The invention discloses a method for extracting 8-acetylharpagide from a decumbent bugle herb plant. An extracting method of which the patent application number is 200510085017 is used for extracting by taking an extract obtained from the decumbent bugle herb plant as a raw material. The method comprises the following steps of: dissolving a raw material into a methanol or ethanol solvent, filtering, and drying a filtrate to obtain a crude extract; and dissolving the crude extract into a specific organic solvent, filtering, recovering a part of the solvent, standing for a certain period of time, precipitating a crystal out, filtering, and repeatedly purifying a precipitate to obtain 8-acetylharpagide of which the purity is over 90 percent. Due to the adoption of the method, the purity of the 8-acetylharpagide serving as a main active ingredient is improved on the basis of an original patent; and the method has the advantages of stable process, high repeatability, easiness for operating and suitability for industrial production.
EP1255547B1 Controlled-release compositions containing opioid agonist and antagonist Controlled-release dosage forms containing an opioid agonist; and opioid antagonist; and a controlled release material release during a dosing interval an analgesic or sub-analgesic amount of the opioid agonist along with an amount of said opioid antagonist effective to attenuate a side effect of said opioid agonist. The dosage form provides analgesia for at least about 8 hours when administered to human patients. In other embodiments, the dose of antagonist released during the dosing interval enhances the analgesic potency of the opioid agonist.
EP1370253B1 Use of alpha, beta unsaturated aryl sulfones for protecting cells and tissues from ionizing radiation toxicity Pre-treatment with α, β unsaturated aryl sulfones protects normal cells from the toxic side effects of ionizing radiation. Administration of a radioprotective α, β unsaturated aryl sulfone compound to a patient prior to anticancer radiotherapy reduces the cytotoxic side effects of the radiation on normal cells. The radioprotective effect of the α, β unsaturated aryl sulfone allows the clinician to safely increase the dosage of anticancer radiation. In some instances, amelioration of toxicity following inadvertent radiation exposure may be mitigated with administration of α, β unsatured arylsulfone.
EP1577311A1 Salts of a pyridazino aquinoline derivative and use for the treatment of pain A compound, 7-chloro-4-hydroxy-2-(2-chloro-4-methylphenyl)-1,2,5,10-tetrahydropyridazino[4,5-b]quinoline-1,10-dione, pharmaceutically-acceptable salts thereof, a method for treating pain comprising administration of a pain-ameliorating effective amount of the compound and pharmaceutical compositions containing the compound are disclosed.
WO2007030721A3 Processes for the preparation of (3r,4s)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((s)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-l-(4-fluorophenyl)-3- (3-(4-fluorophenyl)-3-oxopropyl)-2-azetidinone (Compound 2a). The invention further encompasses processes tor preparing Compound 2a from Compound 1. The invention also encompasses processes for preparing a compound having Formula (A) from a compound having the formula (B); wherein R is selected from the group consisting of: H or a hydroxyl protecting group. The invention also encompasses processes for preparing Compound 2a, preferably to form Compound 2a-Form 01. Also included are processes for preparing ezetimibe from Compound 2a-Form 01 or Compound 2a prepared according to the invention, compositions containing such ezetimibe, and methods for reducing cholesterol using such compositions.
EP2125831B1 Oxazinyl isoflavonoid compounds, medicaments and use The invention provides oxazinyl isoflavonoid compounds and compositions containing same, methods for their preparation and their use as therapeutic agents particularly as cardioprotective, anti-inflammatory, anti-oxidant and chemotherapeutic agents.
CN103301125A Levorotatory pantoprazole sodium composition for injection The invention provides a levorotatory pantoprazole sodium composition for injection, and relates to the technical field of medicine manufacturing. The main medicine of the composition comprises levorotatory pantoprazole sodium and melatonin, wherein the melatonin comprises a quick release part and a cyclodextrin-included slow release part. According to the levorotatory pantoprazole sodium composition for injection provided by the invention, the therapeutic effect of levorotatory pantoprazole sodium is improved, instability caused by oral administration of MT (Melatonin) is avoided and MT is quick to distribute and eliminate and the like, and the first pass effect of MT is reduced. The dosage of levorotatory pantoprazole sodium is reduced, and the side effect of levorotatory pantoprazole sodium is reduced. The design of dosage combining quick release and slow release is in accordance with secretion characteristic of MT, so that the problem of half-life period of MT is solved and the bioavailability of melatonin is improved. Melatonin combined with levorotatory pantoprazole sodium can be used for effectively inhibiting the secretion of gastric acid, so that the composition has a good synergistic effect for treating benign active gastric ulcer.
CN101843667A Shuanghuanglian medicinal composition and preparation method thereof The invention provides a Shuanghuanglian medicinal composition. A method for preparing the Shuanghuanglian medicinal composition comprises the following steps of: mixing and extracting honeysuckle and fructus forsythiae to obtain a honeysuckle and fructus forsythiae extract; extracting scutellaria baicalensis to obtain a scutellaria baicalensis extract; and mixing the honeysuckle and fructus forsythiae extract and the scutellaria baicalensis extract to obtain the Shuanghuanglian medicinal composition, wherein the weight ratio of the honeysuckle to the fructus forsythiae to the scutellaria baicalensis is 1:2:1; and the medicinal composition comprises the following components in percentage by weight: 20 to 40 percent of total flavone, 5 to 20 percent of total saponins, 20 to 30 percent of total organic acid, 8 to 18 percent of saccharides, 0.2 to 2 percent of total amino acid and 0.35 to 1.0 percent of phillyrin. In the Shuanghuanglian medicinal composition, active ingredients are extracted and separated from the honeysuckle, the fructus forsythiae and the scutellaria baicalensis, the impurities and the inactive ingredients are removed, each active ingredient is proportioned reasonably, and the content of chlorogenic acid and caffeic acid is strictly limited, so that curative effect is ensured and safety is improved.
CN102146062A Thiazolidine neuraminidase inhibitor and application thereof The invention relates to a thiazolidine neuraminidase inhibitor and application thereof. The thiazolidine neuraminidase inhibitor is a compound shown as a formula I and a mixture of an optical isomer, a diastereoisomer and raceme of the compound. The application of the compound shown as the formula I in preparing medicines for preventing or treating diseases related to the activity of neuraminidase is disclosed.
CN1840010A Minipill for treating gastric disease and preparation method thereof The invention provides pellets for treating gastropathy and the preparing process, wherein the pullets comprise vitamin U, aluminum hydroxide, belladonna extract, excipient, crumbling agent, Kollidon, the preparing process consists of sieving, mixing homogeneously, making soft material, granulating, shot-blasting, aeration-drying, and loading into capsules.
EP2168598A1 Method of Treatment Using Ligand-Immunogen Conjugates A method and pharmaceutical composition are provided for enhancing the endogenous immune response-mediated elimination of a population of pathogenic cells in a host animal wherein the pathogenic cells preferentially express, uniquely express or overexpress a binding site for a particular ligand. The invention comprises administering to a host animal harboring the population of pathogenic cells the ligand conjugated to an immunogen capable of activating a toll-like receptor. At least one additional therapeutic factor can be administered wherein the therapeutic factor is a compound capable of stimulating an endogenous immune response wherein the compound does not bind to the ligand-immunogen conjugate
WO2011146804A3 Gm3 ganglioside replacement therapy A method of treating individuals lacking the enzyme GM3 synthase, The method includes the use of purified GM3 ganglioside, derived from natural sources, as a replacement therapy. The GM3 can be administered by multiple routes including injection and intranasal delivery. The GM3 source can be dairy, synthetic or tissue.
US20080317731 Phospholipases, Nucleic Acids Encoding Them and Methods for Making and Using Them The invention provides novel polypeptides having phospholipase activity, including, e.g., phospholipase A, B, C and D activity, patatin activity, phosphatidic acid phosphatases (PAP)) and/or lipid acyl hydrolase (LAH) activity, nucleic acids encoding them and antibodies that bind to them. Industrial methods, e.g., oil degumming, and products comprising use of these phospholipases are also provided.
EP2464347A1 Combinations of vascular disrupting agents with inhibitor of apoptosis proteins antagonists The invention relates to combinations comprising a vascular disrupting agent (VDA) with IAP antagonists, for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of proliferative diseases.
DE102006018972A1 Agent, useful for topical treatment of skin disease e.g. psoriasis, neurodermatitis and eczema, comprises coal tar solution, a component of talc, bismuth gallate or sulfur fine-particles, surfactant and optionally carriers or diluents Agent for topical treatment of skin disease comprises 0.1-90 wt.% of coal tar solution, 0.1-40 wt.% of at least a component such as talc, bismuth gallate and sulfur fine-particles, optionally liquid/solid carrier or diluents, and surfactant. - ACTIVITY : Dermatological; Antiinflammatory; Antipsoriatic; Antipruritic; Immunosuppressive; Antiallergic; Vasotropic. - MECHANISM OF ACTION : None given.
US20090149516 desoxyepothilone A and B; Fludelone; anticarcinogenic agents; drug resistance; water solubility for formulability; industrial scale; cytotoxic or growth inhibitory effects on CAG myeloma cells lines; ability to polymerize tubulin; minimum toxicity; isomerization of the double bonds in the ring The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).
US20050222259 Methods of activating PPAR-alpha nuclear receptors in mammals The use of a composition comprising an unsaturated fatty acid which activates the nuclear receptor PPAR-alpha for the manufacture of a dietary supplement, a functional food, or a medicament for reducing appetite or food intake is disclosed. The preferred substances are conjugated fatty acids especially conjugated linoleic acid.
CN102488660A Sustained-release pellet containing pirfeudone The invention discloses a sustained-release pellet containing pirfeudone. The sustained-release pellet is prepared from 15-90 percent by mass of pirfeudone and the balance of pharmaceutically-acceptable auxiliary materials. Due to the adoption of the sustained-release pellet containing pirfeudone, the blood concentration can quickly reach treatment concentration, acting time can be kept for a long time, the blood concentration is stable, the phenomenon of 'peak valley' existing in ordinary preparation release is avoided, the sustained-release pellet has a more durable medicament effect, high bioavailability, low toxic and side effects and a more stable curative effect and is convenient to take, the taking times can be reduced from three times a day to one time or two times a day, the medicament taking compliance of a patient is enhanced, and the probability of abuse and outage is lowered.
WO2014015107A1 Dosing regimen for janus kinase (jak) inhibitors The present invention provides a method for treating allergic dermatitis, atopic dermatitis, or one or more symptoms thereof in a mammal in need, which method comprises administering to the mammal a first therapeutically effective dose of a Janus Kinase (JAK) inhibitor twice a day for a number of days sufficient to ease or eliminate one or more clinical signs in the mammal, followed by a second therapeutically effective dose of the JAK inhibitor at a reduced frequency.
US7169793 An amorphous form of esomeprazole, and dosage forms thereof; enantioselective process involves forming a transition metal complex; treating gastric disorders such as ulcers A process of preparation of optically pure or optically enriched isomers of omeprazole and structurally related sulfoxides is provided. Also provided are an amorphous form of esomeprazole, as well a pharmaceutical composition containing it and a method of using it for treatment of gastric disorders.
WO2010095041A2 Compositions, methods, and kits for treating influenza viral infections The present invention provides compositions, methods, and kits for treating or preventing a viral infection (e.g., an infection caused by an influenza virus).
US20090005326 Single dose roxithromycin The invention relates to a method of treating a bacterial infection in an animal by administering a single dose of roxithromycin.
EP2547339A1 Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions The present invention relates to combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto.
US20100063097 Azabicyclo [3.1.0] Hexane Derivatives as Modulators of Dopamine D3 Receptors The present invention relates to certain azabicyclic compounds of formula (I)′: wherein the several groups are defined herein and are modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
US20120046556 Methods and Kits for Preventing the Spread of Sexually Transmitted Microorganisms This application is directed to methods and kits for preventing the spread of sexually transmitted microorganisms among individuals. The present method is for the application of a medicament comprising an irrigant to an area of the body having, or which may have, a lesion resulting from, for example, a viral, bacteria or fungal infection, thereby damaging the microorganism within the lesion and preventing the organism from infecting human cells.
CA2530116A1 Use of roscovitine for treating lymphocytic leukemia The present invention relates to the use of roscovitine, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for treating chronic lymphocytic leukemia.
CN102579386A Stable oxiracetam preparation The invention relates to a stable oxiracetam medicinal composition which is characterized by comprising an effective curative dose of novel pyrrolidone nootropic selected from oxiracetam, a medicament stabilizer selected from edetate disodium, ascorbic acid and the like and pharmaceutical acceptable accessories, wherein active ingredients can be effectively prevented from being oxidized and degraded. The invention further provides a method for preparing film coated tablets and hard capsules from the medicinal composition. The stable oxiracetam preparation prepared according to the formula and the preparation method, disclosed by the invention, has high storage stability.
CN101423540A Cytarabin 5'-O-L-valine ester and pharmaceutically acceptable salt as well as preparation and application thereof The invention belongs to the technical field of medicine, and relates to a cytosine arabinoside 5'-O-L-valine ester, pharmaceutically acceptable salts and a preparation method and application thereof. The salts can be the trifluoro acetate, the sulphate, the formate, the acetate, the trichloro acetate, the propionate, the butyrate, the paratoluenesulfonic acid salt, the maleate, the lactate, the phosphate, the mesylate and the like of the cytosine arabinoside 5'-O-L-valine ester. The orally taken cytosine arabinoside 5'-O-L-valine ester can obviously improve the oral administration bioavailability of cytosine arabinoside. The cytosine arabinoside 5'-O-L-valine ester and the pharmaceutically acceptable salts can be used for treating leucocythaemia clinically in the form of oral administration or vein administration.
CN202069887U Chitosan/N-Isopropyl acrylamide multi-hole medicine slow release microsphere The utility model provides a chitosan/N-Isopropyl acrylamide multi-hole medicine slow release microsphere. The shell of the microsphere adopts a porous structure, and the inner layer of the microsphere adopts a multi-core structure. The cores are powder medicine, namely resveratrol or pterostilbene. The shell is chitosan/N-Isopropyl acrylamide graft copolymer. The medicine formed after embedding the resveratrol or the pterostilbene is spheroidal powder with particle size of 15 to 80 micrometers, the dispersivity is excellent, the stability and the biocompatibility of medicine can be improved, and meanwhile, medicine slow release and medicine controlled release are achieved at the same time. The microsphere is low in biocompatibility, has less toxicity, and is helpful to improve the drug therapeutic effect of inner core. The slow release microsphere can be used as slow release powder when the resveratrol or the pterostilbene is wrapped by chitosan/ N-Isopropyl acrylamide.
CN102503886A Agomelatine-isonicotine eutectic crystal and compound and preparation method thereof The invention discloses agomelatine-isonicotine eutectic crystal which has the chemical formula (I). The diffraction angles 2theta can be 10.20 DEG, 14.43 DEG, 15.97 DEG, 17.64 DEG, 18.57 DEG, 19.22 DEG, 19.91 DEG, 20.68 DEG, 21.39 DEG, 21.66 DEG, 21.94 DEG, 23.16 DEG, 24.28 DEG, 24.75 DEG, 25.42 DEG, 29.54 DEG, 29.90 DEG and 30.39 DEG. The agomelatine-isonicotine eutectic crystal is prepared by melting agomelatine and isonicotine and cooling. The agomelatine-isonicotine eutectic crystal is easy to prepare and has low preparation cost.
EP1654229A1 Piperidine derivatives as ccr5 receptor modulators Compounds of formula (I) wherein R1, R2, R3, A and n are as defined; and X is S(O)2 NR4R5 or NR6S(O)2R7; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
CN103272108A Foot washing medicine for alleviating chronic fatigue disease The invention discloses a foot washing medicine for alleviating a chronic fatigue disease. The foot washing medicine is prepared by the steps of taking radix clematidis, cortex acanthopanacis, eucommia ulmoides, teasel root, golden cypress, mirabilite, folium artemisiae argyi, erythrina bark, rheum officinale, spina gleditsiae, Japanese yam, cassia twig, caulis sinomenii, caulis spatholobi, honeysuckle stem and sapanwood as raw materials and grinding the raw materials into 100 to 120-mesh powder. The foot washing medicine has the effects of soothing the liver, regulating vital energy, invigorating the spleen, supplementing vital energy, consolidating the constitution and invigorating the kidney, is suitable for the chronic fatigue disease caused by pressure in modern life, work and society, and has the advantages of convenience in use, definite treatment effect, no toxic and side effects and the like, and the total efficiency reaches 86.0% through clinical treatment effect observation of 135 patients with the chronic fatigue disease.
EP1885364A1 Halogenated quindoline dimers for the treatment of cancer The invention provides quindoline dimers where at least one quindoline moiety is substituted in the 2-position of the quindoline scaffold by an halogen atom. The compounds of the invention show advantageous properties as cytotoxic agents for their use as medicaments against cancer.
WO2008018517A1 Therapeutic and/or preventive agent for disease accompanied by cell overgrowth, and polynucleotide useful as the active ingredient The invention provides a therapeutic and/or preventive agent for a disease accompanied by cell overgrowth, particularly a therapeutic and/or preventive agent for the disease with reduced side effects. More particularly, the invention provides a therapeutic and/or preventive agent for a disease accompanied by cell overgrowth, containing a TAK1-specific inhibitor; an siRNA against TAK1 gene; an siRNA expression vector containing a polynucleotide encoding the siRNA; a pharmaceutical containing the siRNA or the siRNA expression vector; a cell with reduced proliferative capacity, in which the expression of TAK1 has been specifically suppressed, or a tissue containing the cell; and the like.
US6974823 Hydantoin derivative compounds, pharmaceutical compositions, and methods of using same The present invention relates generally to novel hydantoin derivative compounds, pharmaceutical compositions containing such compounds, and methods for their use in preventing and/or treating neurological disorders, including physically damaged nerves and neurodegenerative diseases; for treating alopecia and promoting hair growth; for treating vision disorders and/or improving vision; for treating memory impairment and/or enhancing memory performance; and for treating sensorineural hearing loss by administering such compounds.
CN102949365A Enrofloxacin sustained-release tablets for pets and preparation method for same The invention discloses enrofloxacin sustained-release tablets for pets and a preparation process for the same. The enrofloxacin sustained-release tablets disclosed by the invention are stable in medicine release and safe in medication, as well as is composed of enrofloxacin, a sustained-release or controlled-release material, a filler, an adhesive, a lubricant and a flavouring agent. The enrofloxacin sustained-release tablets prepared by the preparation process disclosed by the invention have the characteristics of being convenient to administrate, lasting in action and stable in curative effect.
US20070265253 non-steroidal antiinflammatory agents such as 4H-Pyrido[2,3-g][1,4]benzothiazine-5,10-dione-1,1-dioxo-7-carboxylic acid, useful for treating inflammatory diseases or disorders The invention relates to compounds of formula (I) or formula (II) which have anti-inflammatory activity and comprise a new class of NSAIDs. The compounds are therefore useful for treating inflammatory diseases or disorders. The invention also relates to pharmaceutical compositions containing these compounds, as well as methods of treating inflammatory diseases or disorders using compounds of formula (III) or formula (IV).
WO2012105872A1 Homo- and hetero-polyamino-acid derivatives of fullerene с60, method for producing same, and pharmaceutical compositions based on said derivatives The invention relates to the pharmaceutical industry and to medicine, specifically to novel homo- and hetero-polyamino-acid derivatives of fullerene С60 of general formula: C60(H)x{NH(CH2)nCOO-}x{NH3 +(L)COOH)}x, where n = 2-5, х = 3, L = -(СН2)m, where m = 1-5, or -CO(CH2)kCH(NH2)-, where k = 1-2, characterized in that the compounds comprise covalently bonded amino-acid groups and polar ionic forms of the amino acids, and also to a method for producing said derivatives, and to the production of pharmaceutical compositions based on same. The method for producing homo- and hetero-polyamino-acid derivatives of fullerene is based on the reaction of a nucleophilic bond of amino acids to fullerene, forming covalently bonded amino-acid derivatives of fullerene, with the subsequent introduction of polar ionic forms of the amino acids. A pharmaceutical composition comprises, as active substance, homo- and hetero-polyamino-acid derivatives of fullerene of formula C60(H)x{NH(CH2)nCOO-}x {NH3 +(L)COOH)}x, where n = 2-5, х = 3, L = -(СН2)m, where m = 1-5, or - CO(CH2)kCH(NH2)-, where k = 1-2.
US20110152283 Crystalline pimobendan, process for the preparation thereof, pharmaceutical composition and use The invention relates to a pharmaceutical composition containing pimobendan as an active ingredient. The invention also relates to a crystalline form of pimobendan, as well as to a combination of said crystalline form with at least one other therapeutically active ingredient. Moreover, the invention relates to uses of said crystalline form, as well as to a pharmaceutical composition containing it. Finally, the invention relates to a process for preparing a crystalline form of pimobendan.
US20110263665 Formulations comprising an anti-microbial composition The present invention describes a formulation comprising: (A) at least one surfactant; and (B) an anti-microbial composition that comprises (i) an anti-microbial agent with surfactant properties; (ii) a hydrophobic material and (iii) a polar solvent.
CN102670635A Novel application of icariin to resisting of oxygen deficiency The invention relates to a novel application of icariin to resisting of oxygen deficiency. Proved by the test in the invention, the icariin has remarkable protecting functions for resisting oxygen deficiency induction and oxygen deficiency damage. The invention also provides an application of the icariin to preparation of a medicinal preparation with an oxygen deficiency resisting function.
WO2008035535A1 Capsule including antibacterial agent and artificial joint having the capsule attached thereto Disclosed is a capsule including an antibacterial agent, which can release the agent slowly at a desired rate and can retain the agent in large quantity. Also disclosed is an artificial joint having the capsule attached thereto. The capsule includes an antibacterial agent, is composed of a porous material, and can be attached to at least a part of an artificial joint to release the antibacterial agent included therein into a joint capsule or a bone slowly through the porous material.
US20070293515 1,3-Disubstituted Heteroaryl Nmda/Nr2b Antagonists Compounds represented by Formula I: (wherein A, B, D, P, Q, R1, R2, R3, W and Y are described herein) or pharmaceutically acceptable salts thereof, are effective as NMDA/NR2B antagonists useful for treating neurological conditions such as, for example, pain, Parkinson's disease, Alzheimer's disease, epilepsy, depression, anxiety, ischemic brain injury including stroke, and other conditions.
CA2815542A1 Use of a spironolactone-based composition that exhibits an inhibitory action on t-lymphocyte activation which is useful for preventing and/or treating multiple sclerosis The present invention relates to the use of spironolactone for the preparation of a pharmaceutical composition intended for preventing and/or treating multiple sclerosis. Furthermore, the invention relates to the use of spironolactone directly in T-lymphocytes or dendritic cells obtained from a blood sample taken from the patient and then injected back into the circulation. Therefore, the present invention relates to the use of a composition that comprises spironolactone that can be used in the treatment of multiple sclerosis, which covers the administration of spironolactone directly or of lymphocytes pre-treated with spironolactone, or dendritic cells to individuals requiring such treatment. Spironolactone is an orally administered drug that is less expensive than many of the treatments available for MS and, furthermore, has the advantage of being a known compound already used in humans over extended periods and therefore the adverse effects thereof have been described in clinical studies.
WO2011010083A1 Indolyl-pyridone derivatives Compounds of formula (I) are inhibitors of Chk1, useful in the treatment of, inter alia, cancers: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxy methyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, -N(R11)-R12, -AIk-N(R11)-R12, -0-AIk-N(R11)-R12, -C(=O)OH, carboxy-(C1-C3)-alkyl, or -C(=O)-NH-R13; AIk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from -C(=O)-N(-R16)- or -N(-R17)-C(=O)-; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is an optionally substituted 5-membered monocyclic heteroaryl ring.
WO2012059090A4 Etacrynic acid for use in the treatment of food sensitivity disorders The invention relates to the use of etacrynic acid of the formula (I) for the prophylaxis and treatment of food sensitivity disorders, food intolerances and skin diseases and in particular coeliac disease, and to compositions comprising etacrynic acid.
EP1599432A1 Adamantane derivatives, processes for their preparation and pharmaceutical composition containing them The invention provides compounds of formula (I) in which m, n, R?1, R2, R3, R4 and R5¿ have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
CN101367802A Beta-kabarin alkaloids in quassia wood, preparation method and application thereof The present invention provides beta-kabarin alkaloid in India quassiawood, a preparation method thereof and an application thereof. The alkaloid has a structure as shown in Formula (I). In the preparation method, the plant India quassiawood is used as a raw material, an organic solvent and/or water are/is used for extraction, the chromatographic method and/or extraction method are adopted for separation, and the beta-kabarin alkaloid can be produced. The beta-kabarin alkaloid can be used as anti-inflammation medicine for preventing or treating inflammation caused by the releasing of nitrogen monoxide, tumor necrosis factor-alpha and interleukin-6 inflammation medium.
CN102702119A Pharmaceutical combinations of an angiotensin receptor antagonist and an NEP inhibitor A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.
US20090124652 Polymorphs of 1-(2-Methylpropyl)-1H-Imidazo[4,5-C][1,5]Naphthyridin-4-Amine Ethane-Sulfonate The invention provides various crystalline forms of 1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine ethanesulfonate, pharmaceutical compositions, methods of making, and methods of use.
US7217429 Preventing the drug breakdown due to abnormal secretion of gastric acid, coatings comprising non-alkaline water-soluble cellulose such as hydroxypropylmethyl cellulose or hydroxypropyl cellulose The pharmaceutical dosage form consists of a plurality of units containing a benzimidazole compound labile in an acid medium as the active principle, each unit being comprised of an inert core, a layer containing the active principle and an intermediate layer. These units, mixed with compression excipients, compressed and coated with an enteric coating, provide a tableted pharmaceutical dosage form suitable for oral administration for preventing and treating disorders related to abnormal secretion of gastric acid.
US20120004194 Aldehyde-functionalized polysaccharides Novel aldehyde-functionalized polysaccharide compositions are described that are more stable in aqueous solution than oxidized polysaccharides or other types of polysaccharides containing pendant aldehyde groups. The aldehyde-functionalized polysaccharides may be reacted with various amine-containing polymers to form hydrogel tissue adhesives and sealants that may be useful for medical applications such as wound closure, supplementing or replacing sutures or staples in internal surgical procedures such as intestinal anastomosis and vascular anastomosis, tissue repair, preventing leakage of fluids such as blood, bile, gastrointestinal fluid and cerebrospinal fluid, ophthalmic procedures, drug delivery, and preventing post-surgical adhesions.
US20090029974 Tumor Treatment with Gliotoxin Derivatives The present invention describes the use of Notch2 inhibitors for producing a medicament for the treatment of tumours, which tumours are characterised by ligand-independent Notch2 fragments.
CN103519184A Health care product containing glycyrrhizic acid The invention discloses a health care product containing glycyrrhizic acid. The health care product is mainly prepared through schisandrin B and the glycyrrhizic acid and has exact treatment effects on chemical liver injury.
US20070098757 E-PTFE foil impregnated with an encapsulated bioactive substance A method of impregnating an e-PTFE (expanded polytetrafluoroethylene) foil with a biologically-active substance.
CN102228428B Large volume injection composition containing vinpocetine and preparation method thereof Belonging to the field of pharmaceutical preparation, the invention relates to a large volume injection composition containing vinpocetine and a preparation method thereof. The injection comprises vinpocetine, sodium chloride, acidic amino acid or acidic amino acid salt, L-(+) tartaric acid, a pH value conditioning agent and injection water. According to the invention, acidic amino acid or acidicamino acid salt is chosen as an accessory of the large volume injection composition containing vinpocetine, so that the stability of the large volume injection composition containing vinpocetine and sodium chloride is improved. Meanwhile, in the preparation method of the invention, an operation of introducing carbon dioxide for protection is added during liquid preparation and fine filtration, thus being beneficial to improving the stability of the large volume injection composition containing vinpocetine.
EP1265871B1 Pyridazinyl phenyl hydrazones useful against congestive heart failure Therapeutically active compounds of formula (I) in which R1 to R4 means hydrogen, alkyl, alkenyl, aryl, arylalkyl, carboxyalkyl, hydroxyalkyl or halogenalkyl, or R2 and R3 form a ring of 5-7 carbon atoms, R5 to R9 means hydrogen, alkyl, alkenyl, aryl, arylalkyl, acyl, hydroxy, alkoxy, alkoxycarbonyl, amino, acylamino, alkylamino, aryloxy, halogen, cyano, nitro, carboxy, alkylsulfonyl, sulfonamido or trifluoromethyl, wherein each aryl residue defined above by itself or as a part of another group may be substituted, and pharmaceutically acceptable salts and esters thereof. The compounds increase the calcium sensitivity of contractile proteins of the cardiac muscle and are thus useful in the treatment of congestive heart failure.
WO2005077416A3 Lipid rafts and clostridial toxins The present invention is directed to methods of altering the degree of internalization of a Clostridial toxin; methods of preventing or treating botulinum toxin intoxication; methods of treating metabolic disorders, muscular disorders, nervous system disorders, and/or pain conditions; methods of inhibiting the formation of lipid rafts on cell membranes; methods of treating a disease associated with lipid rafts; and methods of identifying a compound that alters the internalization of a Clostridial toxin.
CN1771959A Famciclovir dripping pill and its prepn The present invention discloses one kind of antiviral medicine composition, and aims at providing one kind of orally taken antiviral famciclovir dripping pill with high bioavailability, fast medicine release, fast acting, high medicine content, easy taking, low cost and production process without pollution. The famciclovir dripping pill is prepared with famciclovir as medicine material and medicine carrier as matrix.
CN1981791A Antibacterial liquid for killing sperma and virus fastly An antibacterial lotion for fast killing sperm and viruses including HIV, gonococcus, chlamydozoan, mycoplasma, herpevirus, syphilis spire, candida, etc in order to prevent the propagation of venereal disease and AIDS is prepared from octylphenyl polyol (0-9), trichlorohydroxy diphenylether, and cnidium fruit. Its preparing process is also disclosed.
EP2654757A1 The use of spinosyns and spinosyn compositions as local anesthetics and as antiarrhythmic agents The present invention relates to the use of spinosyns and spinosyn compositions as local anesthetics and antiarrhythmic agents. Advantageously, spinosyns may be used as local anesthetics and/or antiarrhythmic agents with little or no disruption or harm to the host which may be an animal or human.
US20100010057 Thiazole derivatives as inhibitors of p13 kinase Compounds of formula (I) are inhibitors of P13 kinase activity, and useful in treatment of, inter alia, autoimmune, inflammatory and proliferative diseases: wherein: s is 0 or 1; U is hydrogen or halogen; X is —(C═O), an optionally substituted divalent phenylene, pyridinylene, pyrimidinylene, or pyrazinylene radical, or a bond; P is optionally substituted C1-C6 alkyl and Z is —(CH2)Z—X1-L1-NHCHR1R2; or Z is optionally substituted C1-C6 alkyl and P is —(CH2)Z—X1-L1-NHCHR1R2; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; X1 is (i) a bond; —NR4C(═O)NR5— or —NR4S(═O)2—; or except when X is —(C═O)— (ii) —C(═O)—, —S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z and L1 are as defined in the specification.
CN103284990A Drug with anti-osteoporosis effect The invention discloses a drug with an anti-osteoporosis effect. The drug comprises one, two or more than two of the following components: a compound 1: 5,7,4'-trihydroxyl-3'-methoxy-6,8-dimethyl dihydrhomoisoflavonoid, a compound 2: dihydrhomoisoflavonoid, a compound 3: 6-formyl isoophiopogonone B, a compound 4: 6--formyl isoophiopogonone A, a compound 5: methyl isoophiopogonone B, a compound 6: 5,7,4'-trihydroxyl-6-methyl homoisoflavonoid, a compound 7: 5,7,4'-trihydroxyl-6-methyl dihydrohomoisoflavonoid and a compound 8: methyl dihydrisoophiopogonone A. The drug with the anti-osteoporosis effect provided by the invention has an obvious treatment effect in lowering bone mineral loss of an osteoporosis rat and bone biomechanical strength without an obvious toxic and side effect. The compound source is extensive, not only can be obtained by extracting from the plant, but also can be prepared by adopting an artificial synthesis method.
CN101602786A N*-substituted adenosine derivative, preparation method thereof, drug composition and application The invention discloses an N*-substituted adenosine derivative, a preparation method, a medicine composition and application thereof, in particular relates to an N6-substituted adenosine derivative shown as the general formula (I), two preparation methods of the derivative, a medicine composition using the derivative as effective components, and application of the derivative for preparing medicines and health care products for sedative-hypnotic, anticonvulsion, anti-epileptic, and anti-Parkinson's disease and anti-stupid. The formula (I) is shown in the description.
WO2010002209A3 Novel compounds, isomer thereof, or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist and pharmaceutical compositions containing the same This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
WO2012158117A1 Combination therapies for treating pain This invention generally relates to a combination therapy comprising the use of a substituted benzoimidazole compound and a nonsteroidal anti-inflammatory drug (NSAID) or acetaminophen, and, in particular, to the use of methyl 2-((2-(2,6-difluoro-4- (methylcarbamoyl)phenyl)-5-methyl-1H-benzo[d]imidazol-1-yl)methyl)morpholine-4- carboxylate or a salt thereof and an NSAID or acetaminophen to treat pain. This invention also relates to the combinations themselves, uses of such a combination, and pharmaceutical compositions and kits comprising such a combination.
WO2007017176A8 Wound-healing composition Disclosed are topical formulations containing hyaluronic acid, hydrogen peroxide or other antiseptic agents and optionally adenosine, aminoacids and plant extracts.
US7547697 Alkyl-pyridazine derivatives as 11b-HSD1 inhibitors Compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof for use as pharmaceutical compositions.
CN101843579A 5-hydroxymethyl Tolterodine gel preparation and preparation method thereof The invention provides a 5-hydroxymethyl Tolterodine gel preparation. The 5-hydroxymethyl Tolterodine gel preparation is in external use through being applied and has the transdermal medication effect, and the defects of low bioavailability and many untoward effects of an oral preparation are overcome. The 5-hydroxymethyl Tolterodine gel preparation is mainly prepared from 5-hydroxymethyl Tolterodine, a gel substrate, a filming substrate, an organic silicon elastic body, a transdermal penetration promoting agent, a pH regulating agent, a moisture preserving agent and the like. When the 5-hydroxymethyl Tolterodine gel preparation is in use, the gel preparation contains the filming substrate capable of forming flexible films after being dried, the 5-hydroxymethyl Tolterodine gel preparation is in external use to be applied on the parts of the thigh, the abdomen, the upper arm or the shoulder and the like, can fast form flexible and wear-resistance films on the selected skin regions, and can prevent the gel from being brought away by clothes, at the same time, the medication parts are in a non-sealed state, and the ventilation effect is good. The contained organic silicon elastic body can obviously improve the performance such as the dispersivity, the softness, the wettability, the lustrousness and the like of the gel system, the prepared gel is smooth, translucent and exquisite, the skin has no foreign body sensation after use, the medicine is perpetually and slowly released, the transdermal absorption effect is good, the use is convenient, and the adaptability of the patients can be improved.
WO2009115707A2 Preparation of hydroquinone amide compounds with antioxidant properties. The present invention relates to the preparation of compounds of formula (I) derived from arylacetic acid comprising two phenol functions and an amide function, which have free-radical scavenging and antioxidant properties and which are soluble in lipid media. These compounds can be used as cosmetic and pharmaceutical preparations for the prevention of biological degradations caused by free radicals.
CN102558018A Benzene sulfamide derivative and applications thereof in producing antibacterial drugs The invention relates to a benzene sulfamide derivative and applications thereof in producing antibacterial drugs. The benzene sulfamide derivative can be used for producing new effective drugs against drug-resistant gram-positive bacteria due to the strong inhibiting effect on methicillin-resistant staphylococcus aureus (MRSA), and for producing new antifungal drugs due to the strong synergistic inhibition effect on Candida albicans. The drugs can be used in the form of injection, tablets, pills, capsules, suspending agents or emulsion. The administration route of the drugs can be oral administration, percutaneous administration, intravenous injection or intramuscular injection. The chemical structural formula of the benzene sulfamide derivative is represented as formula (I), wherein R is H, CH3, C2H5 or CH(CH3)2; R' is H, 2-NO2 and 4-NO2; and X is 3-(1-H-indol-3-yl)-, 3-propionyloxy, and 3-propionyloxy (1-3 carbon) ester.
US20110060010 Salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione and derivatives thereof, or polymorphs of salts, process for preparing same and use thereof The present invention provides a pharmaceutically acceptable strong acid salt of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione, a solvate thereof, a process for preparing the same and use in the preparation of a medicament for treating diseases or physiological abnormities by inhibiting inflammatory factors or angiogenesis. The water-solubility of the pharmaceutically acceptable strong acid salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione is quite higher than that of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione. The present invention also provides polymorphs of a pharmaceutically acceptable strong acid salt of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione and a solvate thereof.
CN1657045A Antibacterial medicinal composite containing bota-lactanase inhibitor A composite antibacterial medicine is prepared from beta-lactamase depressant or its medicinal salt or its medicinal ester derivative and cefalotin or cefadroxil through proportional mixing.
US7652031 Compounds which mimic the chemical and biological properties of discodermolide Compounds which mimic the chemical and/or biological activity of discodermolide are provided.
US20120208789 Hydroswellable, segmented, aliphatic polyurethanes and polyurethane ureas Hydroswellable, absorbable and non-absorbable, aliphatic, segmented polyurethanes and polyurethane-urea capable of swelling in the biological environment with associated increase in volume of at least 3 percent have more than one type of segments, including those derived from polyethylene glycol and the molecular chains are structurally tailored to allow the use of corresponding formulations and medical devices as carriers for bioactive agents, rheological modifiers of cyanoacrylate-based tissue adhesives, as protective devices for repairing defective or diseased components of articulating joints and their cartilage, and scaffolds for cartilage tissue engineering.
WO2009032764A1 Acetamide stereoisomer The compound of formula is a water-stable, long acting ß2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.
CN1857594A Medicine composition for activating Qi and relieving hyperacidity to alleviate stomacheache and its preparing method and application The present invention provides a kind of medicine composition for activating Qi and relieving hyperacidity to alleviate stomachache and its preparation process and application. The medicine composition has effective components prepared with cuttlebone 200-270 weight portions, flitilarry bulb 30-40 weight portions, procaine hydrochloride 8.8-10.6 weight portions, corydalis tuber 35-45 weight portions and licorice extract 28-38 weight portions. It is prepared into capsule or medicine powder. The medicine composition is applied in preparing medicine for treating gastric and duodenal ulcer and gastritis caused by stagnation of Qi in gastric cavity.
US20100330173 Compounds and methods for treating influenza This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.
WO2013013417A1 Medicament useful for reducing blood sugar and body weight having the structure of stilbene compounds D isclosed is medicament useful for reducing blood sugar and body weight comprising 5-O-methyl Cajanonic acid A, 5-O-methyl Cajanolactone A or Cajanolactone A and having the structure of the structure of stilbene compounds. Pharmacology experiments have proved that the abovementioned compounds can reduce the fasting blood sugar and body weight, and can be used to prepare the medicament and healthcare food for treating diabetes and adiposity, especially suitable for overweight diabetic patients.
US20130281444 Preparation and pharmaceuticals of biphenyl benzamide-derived derivatives The present invention provides a biphenyl benzamide-derived derivatives, which structure is selected from formula I or formula II: and the synthesis and the application thereof.
EP1514545A1 Use of tolperisone for the treatment of spasms of organes consisting essentially of smooth muscles. Tolperisone (2,4'-dimethyl-3-piperidino-propiophe none) and its acid addition salts are used in combination with excipients and/or carriers to prepare medicaments against painful spasms, tension and/or other disease symptoms relating to organs consisting of smooth muscle. - ACTIVITY - Analgesic; Relaxant; Nephrotropic; Hepatotropic; Uropathic; Respiratory-Gen.; Gynecological; Gastrointestinal-Gen. - No biological data available. - MECHANISM OF ACTION - None given.
CN102641406A Pharmaceutical composition with laxative function and application thereof The invention relates to a pharmaceutical composition with a laxative function, which is an oral preparation mainly comprising the following active ingredients in percentage by weight: 10-50% of fructooligosaccharide, 5-30% of aloe vera whole leaf powder, 10-50% of Semen pruni extract and 5-30% of American ginseng extract. Supplemented by the fructooligosaccharide capable of promoting intestinal peristalsis to strengthen the laxative effect, various drugs are compatible with each other, complement each other, and play a role in toning liver and kidney, clearing heat and moistening intestines, nourishing heart and tranquilizing mind together, so that the purpose of improving constipation is achieved, and the pharmaceutical composition is safe and non-toxic.
CN101700255A Compound fermentation glossy ganoderma capsule and preparation method thereof The invention discloses a compound fermentation glossy ganoderma capsule and a preparation method thereof. The compound fermentation glossy ganoderma capsule is prepared from the main material of fermentation glossy ganoderma bacterium powder and the assistant material of selenium element for enhancing immunity, resisting oxidation and improving sleep quality. The compound fermentation glossy ganoderma capsule is prepared by mixing 70% to 99.6% of fermentation glossy ganoderma bacterium powder, 0.1% to 10% of carrageenin selenide and 0.3% to 20% of magnesium stearate and is prepared into a capsule of the fermentation glossy ganoderma bacterium powder, with the specification of 0.5g/granule. In the compound fermentation glossy ganoderma bacterium powder, the content of glossy ganoderma amylase counted by hyskon) is not less than 8.0g/100g; the content of total triterpene (counted by ursolic acid) is not less than 10.0g/100g; and the content of selenium in the carrageenin selenide is from 19 to 22mg/g. The invention is suitable for preparing and producing the compound fermentation glossy ganoderma capsule.
CN101428034A Antineoplastic combined medicament with enhancing and poison-reducing character The invention relates to an antineoplastic compound medicine having synergism and attenuation effects. The compound medicine mainly comprises teniposide and derivant of arteannuin. Owing to the synergism and attenuation effects in inhibiting the growth of specific tumor cells, the compound medicine is suitable for preparing antineoplastic medicine, particularly for preparing medicines for treating cerebral glioma, liver cancer and cervical carcinoma.
US20070060628 Use of 5-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)benzyl] thiazolidine-2,4-dione Object of the present invention is to search a novel pharmaceutical use of 5-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy) benzyl] thiazolidine-2, 4-dione being a condensed heterocyclic compound, or a salt thereof. 5-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy) benzyl] thiazolidine-2, 4-dione or a salt thereof can exert an excellent effect to promote healing in a dry eye model, and is useful as a therapeutic agent for keratoconjunctival disorders such as dry eyes, corneal ulcer, keratitis, conjunctivitis, superficial punctate keratopathy, corneal epithelial defects, conjunctival epithelial defects, keratoconjunctivitis sicca, superior limbic keratoconjunctivitis and filamentary keratitis.
US20090246280 Resin Powder Containing Aluminum Salt, Process for Production of the Same, and Resin Composition, Phosphorus Adsorbent, Antibacterial Agent or Antifungal Agent Comprising the Same An aluminum salt-containing resin powder of the present invention includes: at lest one matrix resin component selected from regenerated collagen, polyvinyl alcohol and carboxymethyl cellulose; and an aluminum salt. The aluminum salt is chemically bonded to the matrix resin component, and the resultant is powdered. A resin composition of the present invention includes 0.1 wt % or more and 80 wt % or less of the aluminum salt-containing resin powder and 20 wt % or more and 99.9 wt % or less of a resin other than the aluminum salt-containing resin. Thus, the present invention provides an aluminum salt-containing resin powder having a high phosphorus adsorption property, a high antibacterial property and a high antifungal property, and a resin composition containing the aluminum salt-containing resin powder.
US20080161324 Screening for effective drug combinations; single stranded RNA, flaviviridae and/or hepatic viruses; reducing side effects The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E). Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.
US20110064742 Somatostatin Receptor Antagonists and Glucose Control or Hypoglycemia The present disclosure provides methods and uses for controlling tight blood glucose levels in a subject comprising administering an effective amount of a somatostatin inhibitor. The present disclosure provides methods and uses for treating or preventing hypoglycemia in a subject comprising administering an effective amount of a somatostatin inhibitor.
US20080057022 sustained release mixture of polymers, drugs such as antiallergens, antiinflammatory agents or antiseptics, flow control agents and carriers, used for providing relief to discomfort of eyes A composition for providing relief to a discomfort of an eye comprises a pharmaceutically acceptable carrier and a material that allows the composition to remain in an ocular environment for an extended period of time. The composition can further comprise an active ingredient selected from the group consisting of anti-allergic agents, anti-inflammatory agents, anti-infective agents, and combinations thereof.
CN103301189A Medicine for treating seborrhea The invention discloses a medicine for treating seborrhea, which belongs to the technical field of external use medicines for treating seborrhea, and provides the medicine for treating seborrhea to solve technical problems. The adopted technical scheme is that the medicine is prepared from the following raw materials in parts by weight: 220-280 parts of glycerol, 100-200 parts of salicylic acid, 100-200 parts of benzoic acid, 80-120 parts of sophora flavescens, 30-80 parts of povidone lodine, 80-120 parts of fructus cnidi and vanishing cream, wherein the ratio of parts by weight of the salicylic acid to the vanishing cream is 1: (8-10). Generally, the whole formula of the medicine has functions of commonly sterilizing, killing insecticides, diminishing inflammation, relieving itching, killing fungus, astringing and clearing dampness and thus takes effect.
US20100113538 N-hydroxy-4- benzamidine 2 ethansulfonic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}benzamidine 2 ethansulfonic acid salt, a process for the preparation thereof, a pharmaceutical composition for preventing and treating osteoporosis, bone fractures or allergic inflammatory diseases, comprising the same, and an oral formulation for preventing and treating osteoporosis, bone fractures or allergic inflammatory diseases, comprising the same are described.
WO2013131270A1 Scutellarin hydrate and preparation method and use thereof Disclosed is a Scutellarin hydrate of formula C21H18O12·nH2O, wherein n is a number between 1.75-2.0. Also disclosed in the present invention is the preparation method and use thereof. The hydrate has good storage stability, and is suitable for preparing a drug for the treatment or prevention of cardiovascular and cerebro-vascular disease.
US20110190335 Nitrogenated 5-membered heterocyclic compound The purpose of the present invention is to provide a glucokinase activator which is useful as a pharmaceutical agent such as agents for the prophylaxis or treatment of diabetes, obesity and the like, and the like. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
WO2008018140A1 Composition for preventing and/or treating tumor containing component originating in the bark of tree belonging to the genus acacia It is intended to provide a composition which is useful in preventing or treating tumor. Namely, a composition for preventing and/or treating tumor which is characterized by containing a component originating in the bark of a tree belonging to the genus Acacia.
WO2011042765A8 Inorganic salt complexes of vildagliptin The present invention relates to the use of novel vildagliptin complexes for the manufacture of high purity vildagliptin of Formula I and/or pharmaceutical acceptable salts thereof. Further objects of the present invention are pharmaceutically acceptable complexes of vildagliptin and/or amorphous and crystalline forms, anhydrous forms, amorphous and crystalline hydrates, amorphous and crystalline solvates of the complexes and a process for the preparation thereof. Another object of the present invention is the high purity vildagliptin and pharmaceutically acceptable salts thereof prepared form the vildagliptin complexes of the present invention, a process for the preparation thereof and pharmaceutical compositions containing vildagliptin base, pharmaceutically acceptable salts and/or complexes and use thereof for the treatment of type 2 diabetes (NIDDM). The present invention provides pharmaceutically advantageous high purity vildagliptin complexes.
WO2012143703A1 Dibenzothiazepine derivatives and their use in the treatment of cns disorders A compound of formula (I): or a pharmaceutically or veterinarily acceptable salt thereof, or a pharmaceutically or veterinarily acceptable solvate of either entity, wherein: R1, R2, R3, R4, R5, R6, X and m are as defined herein.
WO2009088125A1 A composition for sanitary supplies comprising mucosal immunoadjuvant and a preparation method thereof Disclosed are a composition for sanitary supplies for women (vaginal cleansing solution, vulval cleansing solution, vaginal tablet, etc.) comprising a mucosal immunoadjuvant and a preparation method thereof. Further disclosed are sanitary supplies for women comprising the mucosal immunoadjuvant. The composition of the present invention enhances immunity against infections and diseases by inducing mucosal immunity in the genitourinary system of women, which is susceptible to exposure to infections, thereby further providing an effect of preventing infections and diseases, as well as the intrinsic functions of the sanitary supplies for women.
CN102091089A Application of active burdock oligosaccharide to aquaculture The invention discloses application of active burdock oligosaccharide to aquaculture, particularly the application of the active burdock oligosaccharide serving as an immunopotentiator to aquaculture. The burdock oligosaccharide is natural oligosaccharide which is extracted and separated from burdock root and has better water solubility, better stability and higher purity, wherein the oligosaccharide content is more than 95 percent; the average molecular weight is 2,134Da; 12 furoic fructoses are connected through beta (2-1) glucosidic bonds; the tail end of the burdock oligosaccharide is of a linear straight chain structure that a glucopyranose is connected onto the fructose through an alpha (1-2) glucosidic bond; and degree of polymerization is 13. When the burdock oligosaccharide is used as a growth promoting agent and the immunopotentiator in agriculture, the addition amount of the burdock oligosaccharide accounts for 0.5 to 5.0 percent of the total weight of feeds. The active burdock oligosaccharide has the beneficial effects of promoting the growth of cultured animals, improving the nutrient constituents of animal bodies and improving the nonspecific immunity and the premunition of the animals, also has high activity in the aspect of resisting bacterial infection, has a simple, convenient and feasible using method and can be suitable for cultivation of various aquatic products.
US20130012530 New Positive allosteric modulators of nicotinic acetylcholine receptor The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.
CN101717413A Chiral ruthenium coordination compound and application of same as anti-tumour medicine The invention discloses a chiral ruthenium coordination compound and an application of the same as an anti-tumour medicine. The chiral ruthenium coordination compound has the following general formula: A-[Ru(bpy)2L](PF6)2, wherein A is delta or lambada; L is tFPIP, IPBP, IPBH or PYNI. The chiral ruthenium coordination compound takes ruthenium as a center metal ion and has a complex ion with a rigid octahedral space structure; in molecules, two dipyridyl base groups are used as an auxiliary ligand; 2-substituted phenyl imidazole [4,5-f][1,10] phenanthroline is used as a main ligand; and the chiral isomer of a metal coordination compound with the structure characteristics has optical rotation. These ruthenium coordination compounds have obvious suppression activity to a liver cancer cell strain BEL-7402 and the like and can be used for preparing the anti-tumour medicine.
EP1305285B1 N-substituted indoles useful in the treatment of diabetes Certain N-substituted indoles having aryloxyacetic acid substituents are agonists or partial agonists of PPAR gamma, and are useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR mediated diseases, disorders and conditions.
EP1357912B9 Photodynamic therapy of occult choroidal neovascularization linked to age-related macular degeneration The invention relates to the selection and treatment of subjects afflicted with occult choroidal neovascular lesions, including subjects with age-related macular degeneration, by use of photo dynamic therapy (PDT).
CA2301503C Pharmaceutical compositions for oral administration of molecular iodine The invention is a method of administering therapeutic iodine for treating a disorder in a mammal. The invention comprises a step of feeding said mammal an effective amount of an oxidant for an iodine species and an iodine reductant which will cause oxidation-reduction reactions upon contact with the gastric juices present in the stomach of the mammal. This is done such that molecular iodine is generated in vivo at a ratio of molecular iodine to total iodine of above at least about 0.8.
WO2014057957A1 Steroid compound, and medicine comprising same Provided are: a novel steroid compound useful for a diagnostic medicine; and a medicine comprising the steroid compound. A steroid compound represented by formula (1) (wherein R1 represents a hydroxy group, a sulfonyloxy-type protected hydroxy group, a halogen atom, a radioactive isotope, or a group containing a radioactive isotope; R2 and R3 may be the same as or different from each other and independently represent a hydrogen atom or a protective group for a hydroxy group; and n represents an integer of 0 to 3 or 5); and a medicine comprising the steroid compound.
CA2149753C Lipid derivatives of phosphonoacids for liposomal incorporation and method of use Lipid-containing prodrugs are provided for treating viral infections duo to herpes, influenza, hepatitis B. Epstein-Barr, and varicella-zoster viruses, as well as cytomegalovirus and derivatives of antiviral agents. The compounds comprise phosphonoacids having antiviral activity which are linked, either through the phosphate group or carboxyl group of the phosphonoacid, to one of a selected group of lipids.Phosphonoacetic acid and phosphonoformic acid are thus linked to phospholipids, glycerolipids, sphingolipids, glycolipids, or fatty acids.The compounds persist, after intracellular hydrolysis, as the antiviral phosphonoacids. The lipid prodrugs are effective in improving the efficacy of antiviral phosphonoacids by prolonging their antiviral activity following administration.
US20090324757 Compositions and Methods for Modulating Visceral Sensation and/or Gastrointestinal Reflex Activity The invention relates to compositions capable of modulating visceral sensation and/or gastrointestinal activity obtained from botanical sources. More specifically, the invention relates to compositions comprising an extract product of an Asclepias plant, and methods of modulating visceral sensation and/or gastrointestinal activity in an individual using same.
US20090203588 Outcome prediction and risk classification in childhood leukemia Genes and gene expression profiles useful for predicting outcome, risk classification, cytogenetics and/or etiology in pediatric acute lymphoblastic leukemia (ALL). OPAL1 is a novel gene associated with outcome and, along with other newly identified genes, represent a novel therapeutic targets.
EP1610783A2 Modulation of cell death A method of modulating cell death includes administering pyridoxal-5'phosphate, pyridoxal, pyridoxine, pyridoxamine, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxal-4,5-aminal, pyridoxine phosphonate analogues, or pharmaceutical compositions thereof.
WO2012026662A1 Composition including undecylenic acid and/or conjugated linoleic acid for the prevention and treatment of degenerative neurological disorders The present invention relates to a composition including undecylenic acid and/or conjugated linoleic acid for the prevention or treatment of degenerative neurological disorders including Alzheimer's disease, to a composition for inhibiting calpain activity, and to a method for inhibiting calpain activity. The composition according to the present invention includes at least one fatty acid selected from undecylenic acid and conjugated linoleic acid as an active ingredient, and exhibits the effects of inhibiting calpain activity, and can thus be useful for the prevention and treatment of degenerative neurological disorders including Alzheimer's disease.
US20070293436 Cytoprotective thereapeutic agents for the prevention of reperfusion injury following ischemic stroke The present invention relates generally to the use of γ-glutamyl antioxidants, particularly γ-glutamyl-cysteine, as cytoprotective agents to prevent reperfusion injury (i.e., hemorrhagic transformation) of the blood-brain barrier during reperfusion following an ischemic stroke. The γ-glutamyl antioxidants can be used alone or used in combination with an agent which inhibits the reverse movement of Na/Ca exchange in the blood-brain barrier such as 2-[2-[4-(4-nitrobenzyloxy)phenyl]ethyl]isothiourea methanesulphonate (KB-R7943).
CN1907267A Chlorhydric acid pirenzepine solid preparation for eye-dripping and matching dissolvent thereof The invention discloses an alcaine flat sour solid agent of eye and allocating solvent, which is composed of one of alcaine flat sour, filler, addictive and disintegration agent, wherein the eye drop is allocated by mated solvent, pure water, pH adjuster, osmotic pressure modifier, adhering modifier and conservative through swaying evenly.
CN102197863A Chitosanoligosaccharide capsule The invention discloses a chitosanoligosaccharide capsule. The capsule comprises main materials of chitosanoligosaccharide with molecular weight of 600, ginkgo extract, and mythic fungus extract; and raw adjuvants of starch and magnesium stearate. The preparation comprises, by weight: chitosanoligosaccharide, ginkgo extract, mythic fungus extract, starch, and magnesium stearate. The production technology of the capsules comprises steps of: sieving, weighing, mixing, capsule filling, polishing, selecting, inner packaging, outer packaging, checking, and warehousing. After the processes, a health-care food is produced. The capsule provided by the present invention has an advantage that: the main components of the capsule are chitosanoligosaccharide, total flavonoids, ganoderma lucidum polysaccharid, and ginkgo extract. The capsules are orally taken 2 times a day, and 3 capsules each time. The capsule has a substantial effect in improving comprehensive immune function.
CN101856333A Freeze-dried powder injection of cefamandole nafate and preparation method thereof The invention relates to a freeze-dried powder injection of cefamandole nafate, which is obtained by packaging bulk pharmaceutical of the freeze-dried powder injection of cefamandole nafate according to dosage. The bulk pharmaceutical of the freeze-dried powder injection of cefamandole nafate are obtained by the following steps: dissolving the bulk pharmaceutical of cefamandole nafate with water, filtering with a film of 0.22mu m-1.0mu m, and putting the filtered solution into a freeze dryer for freeze drying. The invention adopts the filtration method to reduce the content of cefamandole in the bulk pharmaceutical, and causes the content of cefamandole nafate to be more than 95%; the process of freeze drying is carried out to obtain new bulk pharmaceutical chemicals; and the new bulk pharmaceutical are directly packaged respectively in accordance with the dosage so as to obtain the freeze-dried powder injection of cefamandole nafate. The obtained injection has good solubility, meets the requirements on all indexes in pharmacopeia, does not contain sodium carbonate and can not generate carbon dioxide, thereby solving the problems in the using process. The freeze-dried powder injection of cefamandole nafate obtained by the invention has good stability and high dissolving speed, merely contains a minute amount of cefamandole, can not influence the dissolvability, is not in need of adding sodium carbonate, and is directly packaged.
CN1718181A Medicine of (4-alkynyl)-aromatic keto-acid compounds for treating chronic obstructive lung diseases A medicine for treating chronic obstructive lung diseases contains (4-alkynyl)-arylketo-acid compounds and the pharmacologically acceptable carrier. Its synthesizing process is also disclosed.
CN102614289A Medicine for treating burning and scalding The invention discloses a medicine for treating burning and scalding, which is a medicine composition prepared by adopting pure natural plants and animals as raw materials through elaborate processing according to certain process. Large amount of clinical application prove that the medicine has particularly remarkable curative effects on fire burning, water scalding, electricity scalding and the like, is short in treatment time and good in curative effect, no toxic and side effects exist in the treatment, scars are not left after heal, the raw materials of the medicine for treating the burning and scalding are wide in raw material source and low in cost, and a preparation method is simple.
WO2014057103A1 Inhibitors of viral replication, their process of preparation and their therapeutical uses Inhibitors of viral replication of formula (I), their process of preparation and their therapeutical uses. The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.
CN101007016A Drug for interventional and targeting perfusion therapy of lumbar and cervical disc protrusion and its proportion The invention provides a medicament for the treatment of waist-neck disc-projection disease through inserted targeting perfusion method, which comprises 0.9% physiological saline solution 250-500ml, vitamin C 5.0g, vitamin B1 300mg, vitamin B6 300mg, vitamin B12 200ug, corenalin 1.0g and Triamcinolone Acetonide 40mg.
US20110020272 Combination therapy for treating hepatitis viral infection Disclosed are methods of using proteasome inhibitors (PI) in combinations with other pharmaceutically active agents for treating viral hepatitis infections, for example, for treating therapy-resistant and -refractory viral hepatitis infections. Also disclosed are pharmaceutical compositions and kits of pharmaceutical compositions which can be used for treating viral hepatitis infections, for example, for treating therapy-resistant and refractory viral hepatitis infections.
CN101732313B Medicine composition of naloxone hydrochloride and polyethylene glycol and preparation method thereof The invention belongs to the technical field of medicine, which discloses a medicine composition of naloxone hydrochloride and polyethylene glycol and a preparation method thereof. The weight percent of the naloxone hydrochloride to the polyethylene glycol of the composition is 1:0.1-10. The invention solves the problem that naloxone hydrochloride injection in the prior art is unstable to light, is convenient to master the application quantity and the effective dose and enables the clinical application to be safer and more effective.
CN103550201A Schisandra chinensis preparation The invention discloses a schisandra chinensis preparation. The preparation is prepared from raw materials including schisandrin A and schisandrin B. The preparation has actual therapeutic effects for different types of liver injuries.
US20110070575 Immunomodulatory Compositions, Combinations and Methods The invention provides immunomodulatory compositions, immunomodulatory combinations, and methods of modulating TLR7-mediated biological activity. Generally, the immunomodulatory compositions include an immunomodulatory oligonucleotide in an amount effective to reduce TLR7-mediated biological activity. In some cases, an immunomodulatory combination can further include an IRM compound. In some of these embodiments, the IRM compound can be a TLR7/8 agonist. Generally, the Imethods include contacting immune cells with an immunomodulatory composition in an amount effective to reduce TLR7-mediated biological activity.
US20110224268 Compositions and methods of using R(+) pramipexole Pharmaceutical compositions of R(+) pramipexole and methods of using such compositions for the treatment or prevention of diseases associated with or related to mitochondrial dysfunction or increased oxidative stress are disclosed.
CA2772261A1 Novel nucleoside phosphonates and analogs Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are nucleoside phosphonates and esters thereof.
US7211586 Substituted tetrahydroisoquinolines The invention is directed to physiologically active compounds of formula (I): wherein: R1 represents optionally substituted aryl, optionally substituted heteroaryl, R3NH—Ar1—L2— or R3—NH—C(═O)—NH—Ar2—L2—; R3 represents aryl or heteroaryl; Ar1 represents a saturated, partially saturated or fully unsaturated 8- to 10-membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Ar2 represents aryldiyl or heteroaryldiyl; L1 represents a linkage, such as an alkylene linkage; L2 represents an alkylene chain linkage; R2 represents hydrogen, halogen, C1-4alkyl or C1-4alkoxy; and Y is carboxy or an acid bioisostere; but excluding compounds where an oxygen, nitrogen or sulfur atom is attached directly to a carbon carbon multiple bond of an alkenylene or alkynylene residue; and the corresponding N-oxides and ester prodrugs thereof, and the pharmaceutically acceptable salts and solvates of such compounds, and the N-oxides and ester prodrugs thereof. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).
CN1615877A Mosapride citrate oral solution The present invention discloses a kind of orally taken mosapride citrate solution superior to common mosapride citrate tablet in that it has fast absorption, short period of reaching peak medicine concentration in blood, easy taking by old people and high bioavailability. When being taken after meal, it can eliminate the digestive tract symptoms of ructus, nausea, abdominal flatulence, etc. Mosapride citrate in water solution is light and heat unstable, and the present invention prepares orally taken mosapride citrate solution with rather stable property via adding glycerin, alcohol, propylene glycol, polyglycol-300, polyglycol-400, etc. as essential supplementary material. The present invention also contains certain amount of preservative and corrective.
WO2014146699A1 Antagonists of the cannabionoid receptor cb1 for use in the treatment of diseases associated with neuronal dendritic abnormalities The invention relates to antagonists of the cannabinoid receptor CBI for use in the treatment and prevention of diseases associated with neural dendritic abnormalities, such as Down's syndrome, Angelman's syndrome, Rett syndrome and tuberous sclerosis. More specifically, the invention provides a method of treatment or prevention of such diseases by the administration of the compound rimonabant.
US20080014223 Syrup Composition Comprising Dexibupropen as an Active Ingredient and Method for the Preparation Thereof A dexibupropen syrup composition comprising dexibupropen ((S)-ibupropen) having an average particle size ranging from 10 to 300 μm as an active ingredient, which does not contain glycerine and has a viscosity ranging from 500 to 3,000 cps and pH ranging from 3.0 to 6.0, shows improved safety, uniformity of efficacy, and taste.
CN103495005A Ointment for burn patients and preparation method thereof The invention discloses ointment for burn patients and a preparation method thereof. Active ingredients of the ointment comprise 60-80g of folium isatidis, 40-60g of root-bark of densefruit pittany, 40-60g of herba schizonepetae, 20-30g of camphor, 40-60g of amur corktree bark, 50-70g of garden burnet root, 40-60g of welsh onion leaf, 50-70g of myrrh, 50-70g of fructus sophorae, 40-60g of black soya bean, 10-20g of periostracum serpentis, 40-60g of poria cocos, 40-60g of coptis and 30-50g of borneol. The ointment can solve the problem of local blood stasis and inner retardation, channel and collateral blocking, and toxic heat flourishing and has good effects of promoting blood circulation to remove blood stasis and dredging collaterals, clearing away heat and toxic materials and cooling blood, and treating burn. The ointment has an effective rate of 92.4% and a good effect rate of 89.7%.
US6867211 Fused nitrogen biheterocyclic derivatives; immunomodulaters; inhibiting cytokine release The present invention relates to 4-pyridyl- and 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1: in which the variables have the meanings indicated in the description. The compounds according to the invention have immunomodulating and/or cytokine release-inhibiting action and are therefore utilizable for the treatment of disorders which are connected with a disturbance of the immune system.
EP1537865A1 Use of sulfur containing compounds and proteolytic enzymes for the prevention and therapy of the UDP-Glucuronosyltransferase 1 deficient Type II Diabetes mellitus Prophylaxis and therapy of type II diabetes mellitus due to high toxin concentrations, in turn due to insufficient glucuronidation by uridine diphosphate glucuronosyl transferase 1 (UGT1) and high intestinal production of toxins, involves molecular genetic testing of UGT1 isoenzymes and administering (a) e.g. N-acetylcysteine, glutathione, taurine; (b) pepsin together with citric acid before a protein-rich meal; and (c) lactulose. - Prophylaxis and therapy of type II diabetes mellitus due to excessively high concentrations of essentially excreted toxins, in turn due to insufficient glucuronidation by uridine diphosphate (UDP) glucuronosyl transferase 1 and non-physiologically high production of toxins in the large intestine (designated L-diabetes), carried out as early as possible (at the latest when diabetes mellitus type II is diagnosed), involves: - (1) molecular genetic testing of UDP glucuronosyl transferase 1 (UGT1) isoenzymes (about a dozen of which are known); and - (2) on the basis of established UGT1 insufficiency, due to UGT1A1 deficiency, administering (a) the sulfur compounds N-acetylcysteine, glutathione, taurine, L-cystine L-methionine, L-lysine and L-arginine, (b) pepsin together with citric acid before a protein-rich meal (to reduce the formation of toxins by inappropriate protein digestion in the large intestine) and (c) lactulose (to promote bifidobacteria populating the large intesine). - ACTIVITY - Antidiabetic; neuroprotective; vasotropic; cerebroprotective; antiarthritic. - MECHANISM OF ACTION - Uridine diphosphate glucuronosyl transferase 1 isoenzyme activity stimulant; protein digestion modulator.
EP2685966A1 Controlled release pharmaceutical compositions of selective serotonin reuptake inhibitor The present invention provides a controlled release pharmaceutical composition comprising selective serotonin reuptake inhibitor and a process for preparation thereof. The controlled release pharmaceutical composition comprises: a deposit-core comprising a selective serotonin reuptake inhibitor, one or more controlled release agent(s) and one or more pharmaceutically acceptable excipient(s), a support-platform applied to the deposit-core, a controlled release coating and, an immediate release coating comprising a selective serotonin reuptake inhibitor and one or more pharmaceutically acceptable excipient(s).
WO2010059858A1 Manassantin compounds and methods of making and using same Provided are manassantin compounds and methods of using the compounds. Provided are methods of treating a disease, the method comprising administering a compound according to Formula I. Further provided are pharmaceutical compositions comprising compounds according to Formula I. Also provided are methods of inhibiting HIF-1 in a cell, the methods comprising administering to the cell a compound according to Formula I.
US8183352 Attenuated vif DNA immunization cassettes for genetic vaccines The present invention is directed to nucleic acid molecules encoding attenuated, non-functional virion infectivity factor (vif) proteins. The nucleic acid molecules of the invention are inserted into recombinant expression vectors and administered to mammals in order to induce a cellular and humoral immune response to the encoded protein product.
WO2009063241A1 3-hydroxyanthranilic acid or salts thereof1 for treating cancer or infections 24 Abstract This invention relates to a novel inhibitor of indoleamine 2,3-dioxygenase (IDO) and its use in the treatment of cancer or infections, either alone or in combination with additional therapeutic agents.
US20080161402 Targeting the Reverse Mode of the Na+/Ca2+ Exchanger For the Treatment of Neurodegenerative Conditions A method for treating a neurodegenerative condition, in an animal of the mammalian species, including humans, comprising the step of administering to ganglion cells and their axons (optic nerve) of said mammal a pharmaceutical composition which comprises as its active ingredient one or more compounds having activity for blocking a reverse mode of the sodium/calcium exchanger.
CN101322701B Amoxicillin sodium and sulbactam sodium for injection and preparation of freeze-dried injection thereof The invention discloses a preparation method of amoxicillin sodium and sulbactam sodium used for injection and a freeze-dried powder injection thereof as well as a separating and purifying method of the amoxicillin sodium and sulbactam sodium used for injection. By adopting high speed countercurrent chromatography, a solvent system of an immobile phase and a mobile phase prepared from trichloromethane, ethyl acetate, methanol and water is used for separating and purifying amoxicillin sodium and sulbactam sodium to obtain the amoxicillin sodium and sulbactam sodium used for injection; the purity of the obtained product can reach more than 98% and the prepared injection has improved stability.
EP2187886A1 Stable pharmaceutical composition comprising a hydrosoluble vinflunine salt Stable pharmaceutical composition consisting of a hydrosoluble vinflunine salt and at least one diluent and one lubricant, said composition being in the form of a solid intended for oral administration. The hydrosoluble vinflunine salt is preferably Vinflunine ditartrate. The pharmaceutical composition is advantageously in the form of a capsule or tablet. The invention also concerns a method of treating cancer pathology comprising the oral administration of the pharmaceutical composition of the invention.
CN101301294A Combinated inhibitors of FBP-ase and antidiabetic agents for diabetes treatment The invention discloses a pharmaceutical composition that includes at least one insulin secretagogue and at least one FBPase inhibitor of pharmaceutical dosage, wherein the insulin secretagogue is a dipeptidyl peptldase-ó¶ (DPP-IV); and wherein the FBPase inhibitor is combined with AMP site point of the FBPase. The FBPase inhibitor is selected from compounds of chemical formulae I and IA or acceptable pro-drug or salt pharmaceutically. The chemical formulae I and IA are as follows; the invention further discloses use of the pharmaceutical composition to prepare pharmaceuticals that treats diabetes.
US20110039825 Ligands of alpha-adrenoceptors, dopamine, histamine, imidazoline and serotonin receptors and their use The invention relates to novel ligands the broad spectrum of biological activity of which includes simultaneously α-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and serotonin receptors, among them serotonin 5-HT7 receptors, which are compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers, pharmaceutically acceptable salts and/or hydrates, wherein: R1 is a substituent of amino group, selected from hydrogen, optionally substituted C1-C4 alkyl, acyl, heterocyclyl, alkoxycarbonyl, substituted sulfonyl; R2 is a substituent of cyclic system, selected from hydrogen, halogen, optionally substituted C1-C4 alkyl, CF3, CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulfonyl; Ar is optionally substituted aryl not necessarily annalated with heterocyclyl, or optionally substituted aromatic heterocyclyl; W is optionally substituted (CH2)m group, optionally substituted CH═CH group, optionally substituted CH2—CH═CH group, C≡C group, SO2 group; n=1, 2; m=1, 2, 3; solid line accompanied by dotted line, i.e. may represent single or double bond. The invention also relates to active ingredients, pharmaceutical compositions comprising the said ligands as active ingredients; to novel medicaments useful for treatment of diseases and conditions of central nervous system (CNS) of humans and warm-blooded animals.
US7759313 Induction method for cell differentiation The invention relates to peptide derivatives which function as differentiation-inducing factors. The peptide derivatives are useful for treating cancer, particularly melanoma, for increasing the efficacy of melanoma immunotherapy, and for reducing hematological toxicity of chemotherapy.
US20120237457 Anti-bacterial oral care composition and method for producing the same An anti-bacterial oral care composition and method for producing the same are disclosed. The composition comprises chitosan, organic acid, bioflavonoids and xylitol that are mixed together and can effectively inhibit the growth of bacteria in oral cavity, such as 99.9% of staphylococcus aureus, 99.9% of streptococcus mutans, 99.9% of candida albicans, thus reducing the occurrence of decayed tooth. Furthermore, no chemical preservative and anti-bacterial agent are added in the composition, reducing the damage to the oral mucosa and the health of the user.
CN101703653A Medicinal composition for treating oldfracture and bone nonunion and preparation method thereof The invention discloses a medicinal composition for treating oldfracture and bone nonunion, which is prepared from the following raw materials: 0.5 to 1.5g of stiff silkworm, 1 to 3g of bezoar, 0.5 to 1.5g of safflower, 0.5 to 1.5g of frankincense, 0.5 to 1.0g of ephedra herb, 0.5 to 1.5g of cablin potchouli herb, 0.5 to 1.5g of dragon's blood, 1 to 3g of ginseng, 0.5 to 1.5g of clove mother, 0.5 to 1.5g of hematite, 1 to 3g of Chinese eaglewood, 0.5 to 1.5g of sanchi, 1 to 3g of sandalwood, 0.5 to 1.5g of szechuan lovage rhizome, 0.5 to 1.5g of borneol, 0.5 to 1.5g of pyrite, 60 to 120mg of adenosine triphosphate and 0.1 to 0.3g of venoruton. A preparation method thereof comprises the steps of: performing the initial processing of raw materials and the processing of the raw materials; grinding various medicaments after the processing, the adenosine triphosphate and the venoruton into powders, mixing the powders, and then stirring the mixture evenly; and processing the mixture into pills or loading the mixture into capsules. The combination of Chinese and western medicaments can quicken the time of activating blood and nourishing blood, dispersing swelling and relieving pain, and uniting bone, so the medicinal composition promotes blood circulation in shorter time, improve the growth of damaged sclerotin, powerfully promotes the formation of poroma, strengthens the metabolic capability of bone tissues, has stronger effect on tissue repair, is extremely favorable for the growth of the bone tissues, can be used for treating the bone nonunion and the oldfracture caused by various reasons, and has small side effect.
CN101875687B Triterpenoid, and medicinal composition and application thereof in tumor treatment The invention relates to triterpenoid, and a medicinal composition and application thereof in tumor treatment. Experiments of the invention prove that the triterpenoid has the obvious effect of preventing the tumor diseases of a digestion system, and particularly the good effects of preventing colon cancer, rectal cancer, liver cancer and the like. The invention also provides the application of the triterpenoid in the preparation of medicinal preparations for preventing the tumor diseases.
WO2007027118A1 Dermatological composition The invention relates to pharmaceutical agents for protecting the skin from chemical and biological damage effects, from bacterial and fungus infections, for preventing occupational skin diseases, contact dermatitis including allergic dermatitis, for rendering first predoctor aid and for subsequently treating traumatic skin, soft tissue and mucous coat defects. Said invention can be used in industry, building, agriculture, medicine and at home. The inventive therapeutic and remedial dermatological composition for local application contains an active principle in the form of complex compounds of rare-earth element salts and a pharmaceutically acceptable carrier. Said pharmaceutical composition based on complex compounds of rare-earth compositions and polyhydroxy compounds in the form of a liquid or soft dosage form exhibits an expressed protective and preventive, dermoprotective and curative effect, the absence of side reactions, is easily tolerant and rapidly repairs the skin.
WO2010033980A3 4-azaindole bisphosphonates Novel 4-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
WO2007143506A3 Substituted benzimidazole thiophene benzyl ether compounds The present invention provides benzimidazole thiophene compounds of the following formula (I), pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
CN103494776A Tamoxifen citrate freeze-dried powder injection The invention relates to a tamoxifen citrate freeze-dried powder injection which comprises tamoxifen citrate, a composition of sorbitol, dextran and lactose in a weight ratio of 3.2:5.5:2, a composition of arginine and glutathione in a weight ratio of 1.6:5.7, and disodium ethylenediamine tetraacetate.
US7592455 potent and selective inhibitors of p38 kinase, especially p38 alpha , p38 beta and p38 beta 2; immune or inflammatory disorders; Ethyl 3-(benzylamino)-6-oxo-7-phenyl-6,7-dihydrothieno[2,3-b]pyridine-2-carboxylate A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 6-oxo-6,7-dihydrothieno[2,3-b]pyridine ring system, being inhibitors of p38 kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.
WO2013173382A1 Benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein The present invention relates to benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
WO2008079277A1 Certain pyrazoline derivatives with kinase inhibitory activity The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.
US20090186879 Tricyclic compounds and use thereof There is provided a compound of the formula (I′): wherein x is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to 8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.
US7001896 Side effect reduction; antidiabetic agents; using 4-diethylphosphinoylmethyl-N-(-4-bromo-2-cyanopheny)benzamide The present invention provides a pharmaceutical composition for treating diabetes containing 4-diethoxyphosphinoylmethyl-N-(4-bromo-2-cyanophenyl)benzamide, particularly a pharmaceutical composition for treating diabetes that exhibits excellent effects for treating type II diabetes and the prevention of diabetic complications.
CN101020060A Cyclodextrin clathrate of entecavir and its prepn proces and medicinal application The present invention relates to cyclodextrin clathrate of entecavir with molar ratio between entecavir and cyclodextrin of 1 to (0.7-8), preferably 1 to (1-2). The cyclodextrin clathrate of entecavir has high water solubility, high leaching degree and high stability. The present invention is favorable to the medicinal application of entecavir. The present invention also relates to the preparation process of cyclodextrin clathrate of entecavir and its medicinal application.
CN1785172A Transfusion contg. tanshinone II A sodium sulfonate and its prepn. method A perfusion of tanshinone IIA-sodium sulfonate for treating coronary heart disease, angina pectoris, myocardiac infarction and ventricular early heartbeat contains tanshinone IIA sodium sulfonate (0.002-0.16 Wt%), antioxidizing agent (0-20), solubilizer (0-20), osmosis pressure regulator (0.3-75) and the water for perfusion. Its preparing process is also disclosed.
US7960367 Pregnane steroids and their use in the treatment of CNS disorders Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.
CN103446174A Application of mannuronic acid oligomers in preparing medicines, health products or dietary supplements for preventing and treating alcoholic liver injury The invention provides application of mannuronic acid oligomers in preparing medicines, health products or dietary supplements for preventing and treating alcoholic liver injury. Mannuronic acid oligomers with different molecular weights, which are obtained by degrading polymannuronic acid graded and purified from algin, can lower the hepatosomatic index increase caused by alcoholic injury, resist triglyceride and cholesterol increase caused by alcohol, effectively lower glutamic-pyruvic transaminase and glutamic oxaloacetic transaminase increase in serum caused by alcohol, enhance the total oxidation resistance and glutathione level of the serum, lower the mouse drunkenness rate, prolong the mouse drunkenness time, and shorten the sober-up time, thereby implementing the protective action and hangover alleviating function on alcoholic hepatic injury. The products provided by the invention are derived from marine natural products, have the advantages of abundant resources, high industrialization tendency, high safety, high effectiveness and the like, and have wide development and application prospects in the aspects of prevention and treatment of alcoholic hepatic injury, hangover alleviation and liver protection.
US20060222628 Gallium complexes of 3-hydroxy-4-pyrones to treat infection by intracellular prokaryotes and DNA viruses Methods are provided for treating or preventing infections by obligate intracellular prokaryotes, including mycoplasma, rickettsia and chlamydia, and DNA viruses, including herpes viruses, papillomaviruses, adenoviruses and hepatitis B virus. The methods involve the administration of 3:1 complexes of 3-hydroxy-4-pyrones with gallium, e.g., gallium maltolate. Therapies incorporating gallium maltolate in combination with agents used against obligate intracellular prokaryote and DNA virus pathogens are also provided, as are multi-combination therapies designed to treat co-infection by an obligate intracellular prokaryote or DNA virus in an immunocompromised individual. These multi-combination therapies rely on the ability of gallium maltolate to complement antiviral medication regimes against both HIV and other pathogens such as herpesvirus infections, including Kaposi sarcoma, CMV retinitis and blindness, and lymphomas, in patients immunocompromised by HIV infection.
WO2008055092A3 Use of enoxaparin sodium for treating patients with acute ischemic stroke Methods for treating acute ischemic stroke in a patient in need thereof comprising administering an effective amount of enoxaparin sodium to the patient for a therapeutic dosing period are described. Also described are methods for preventing or treating thrombosis, such as thrombotic episodes, in a human patient with acute ischemic stroke by treating that patient with enoxaparin.
CN103524413A Hydrogenated acridine derivative and application thereof The invention relates to the field of chemical synthesis, and particularly relates to a compound with the general formula being Y-L-X and an application of the compound serving as a calcium channel blocking agent or/and an acetylcholinesterase inhibitor. The compound with the general formula being Y-L-X can be used for adjusting calcium homeostasis and treating cardiovascular diseases, stroke or dementia.
CN101138565A Platelet aggregation-against pharmaceutical composition and method of preparing the same The present invention relates to a medicine combination as well as the preparation and purposes, in particular to an anti-platelet aggregation medicine combination including Dextran-aspirin and clopidogrel bisulfate as well as the preparation and purposes. The medicine combination includes the effective dose of Dextran-aspirin and clopidogrel bisulfate. The medicine combination can prevent and treat cardiovascular thrombotic diseases, which is used to inhibit the platelet aggregation, to increase the stability of pharmaceutical preparations, to reduce the side effects on the human gastrointestinal tract, and to improve the patient compliance and drug safety.
CA2607544A1 A pharmaceutical formulation and its use for the treatment of acquired immune deficiency syndrome (aids) and other aids related diseases and a process for its preparation The present invention relates to the pharmaceutical formulation, in particular a substance obtained from purple maguey (Tradescantia Spathacea) plant, for the treatment of Acquired Immune Deficiency Syndrome (AIDS) and other AIDS related diseases, as well as the process of obtaining said pharmaceutical formulation and its use for the treatment of AIDS and other AIDS related diseases.
US20110212959 Cyanoisoquinoline Compounds and Methods of Use Thereof The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure:
US20080015184 Urea Substituted Imidazopyridines, Imidazoquinolines, and Imidazonaphthyridines Imidazopyridine, imidazoquinoline, and imidazonaphthyridine compounds having a urea substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
WO2007071728A1 Hydantoins with insulinotropic action The present invention relates to a hydantoin of general formula I in which R1 and R2 represent, independently of one another, a C1-C6-alkyl group, an aryl group or an aralkyl group; R3 and R4 represent, independently of one another, a hydrogen atom, a C1-C6-alkyl group, an aryl group or an aralkyl group; or, in the case where R4 represents a hydrogen atom: its tautomeric form of general formula Ia in which R1, R2 and R3 are as defined in general formula I, or its tautomeric form of general formula in which R1, R2 and R3 are as defined in general formula I, or pharmaceutically acceptable addition salts, isomers, enantiomers and diastereoisomers thereof, and mixtures thereof. It also relates to a process for the preparation thereof and to the use thereof in the treatment of diabetes.
CN103524460A Sulfanilamide derivative as well as preparation method and application thereof The invention discloses a sulphanilamide derivative shown in general formulas I-V and a preparation method of the sulphanilamide derivative compound. The route is short, degree of commercialization of raw materials is high, the raw materials are available, and the preparation method is simple; the sulphanilamide derivative compound has antibacterial and antifungal activities, can be used for preparing antibacterial and/or antifungal medicines and has a good clinical application prospect.
US20050226884 Using monoclonal antibody as diagnostic and therapeutic tool in treatment and prevention of cell proliferative and degenerative bone disorders; immunotherapy This invention provides methods for detecting cancers and for evaluating the prognosis of cancer patients. In particular, the methods of this invention utilize YKL-40 as a marker for the presence or absence of a cancer and for the prognosis (e.g. likelihood of recurrence) of a cancer. Elevated levels of YKL-40 are indicative of the presence of a cancer in undiagnosed subjects and indicate likely recurrence of the cancer in subjects diagnosed as having a cancer.
CN102552922A Drug combination and preparation method and application thereof The invention discloses a drug combination which comprises a carrier and a drug loaded on the carrier. The drug combination is characterized in that the drug is a fat-soluble drug; the carrier is a poly (aspartic acid-co-lactic acid)-phosphatidyl ethanolamine graft polymer with a structure shown in a formula (1), wherein n is 15 to 30, x is 10 to 120, y is 10 to 120 and z is 10 to 120; A is a base group with a structure shown in a formula (2); and R and R' are respectively alkyl groups with the carbon atom quantity being 15 to 21. The invention also comprises the preparation method and the application of the drug combination. The drug combination, particularly the drug combination carrying paclitaxel, has strong lethality to tumor cells, especially to lung cancer cells, cervical cancer cells and liver cancer cells, and also has sustained release effect and pH value sensitivity.
US20100202977 Modulation of Stat 6 Expression for the Treatment of Airway Hyperresponsiveness Disclosed herein are compounds, compositions and methods for modulating the expression of STAT 6 in a cell, tissue, or animal. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders related to expression of STAT 6, airway hyperresponsiveness, and/or pulmonary inflammation.
CN102988402A Pharmaceutical composition containing adenosine cyclophosphate compound and preparation method of pharmaceutical composition The invention relates to a pharmaceutical composition and particularly relates to a pharmaceutical composition containing adenosine cyclophosphate compound and a preparation method of the pharmaceutical composition. The composition contains adenosine cyclophosphate and sodium bicarbonate in a weight ratio of 1:(0.05-0.5), preferably 1:(0.1-0.25). The adenosine cyclophosphate is a crystalline compound; and an X-ray powder diffraction diagram of the crystalline compound, which is obtained by measuring through Cu-Ka rays, is as shown in a figure 1. The dosage form of the composition is hydro-acupuncture or lyophilized powder injection, preferably lyophilized powder injection. The pharmaceutical composition prepared by the invention is safe and stable and can satisfy the need of the clinical medication.
WO2010020548A1 Glyt1 receptor antagonists The present invention relates to a compound of the general formula (I) wherein R1/R2 are independently from each other lower alkyl, or form together with the N-atom to which they are attached a heterocyclic group, selected from pyrrolidine, piperidine, piperazine, 4-methyl-piperazine, 4-cyclopropyl-piperazine, thiomorpholine, morpholine, 1-(3-oxa-8-aza- bicyclo[3.2.1]oct-8-yl or 1-(2-oxa-6-aza-spiro[3.3]hept-6-yl; X is a bond, -CH2- or -O-; Ar1 is aryl or heteroaryl, which are unsubstituted or substituted by one or two substituents selected from halogen, lower alkyl, lower alkoxy, or lower alkyl substituted by halogen; Ar2 is aryl or heteroaryl, which are unsubstituted or substituted by one, two or three substituents selected from halogen, lower alkyl, lower alkoxy, hydroxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, benzyl or phenyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to their corresponding enantiomers and/or optical isomers thereof. It has surprisingly been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GIyT-1), and that they have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.
WO2008022747A1 Tricyclic lactam derivatives, their manufacture and use as pharmaceutical agents Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
US20090291153 Health food, Method for producing the same and dried Product and Extract Conophylline, contained in leaves of Ervatamia microphylla or Tabernaemontana divaricata, can induce non-tumor cells to differentiate into insulin-producing cells and thereby to produce insulin and also to lower blood glucose levels. Thus, in the present invention, dried products and extracts of leaves of Ervatamia microphylla or Tabernaemontana divaricata, which contain conophylline, are used as health foods for preventing and improving diabetes and obesity or health foods for lowering blood glucose levels.
US7148222 Substituted pyrido-pyridazine derivatives which enhance cognition via the GABA-A receptors The present invention discloses a compound of formula 1, or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, —CO2Ra, —CONRaRb or —CRa&═NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; a pharmaceutical composition comprising it; its use in a method of treatment; use of it to manufacture a medicament; and a method of using it to prevent or treat anxiety, convulsions or cognitive disorders.
CN1726922A Usage of stigmastane-3,5,6-alcohol and derivative for preparing antiviral remedy, and new stigmastane-3,5,6-derivative of tri-alcohol An application of stigmastane-3,5,6-trio. And its derivative in preparing the medicines to treat AIDS and hepatitis B, a novel stigmastane-3,5,6-triol derivative, and their medicinal composition are disclosed.
US20100112053 Gastric retention-type sustained-release levodopa preparation The present invention is to provide a levodopa preparation which is able to persistently release levodopa in the stomach, has a sufficient gastric residence time, is in an easily ingestible size and is able to be easily manufactured industrially with an object of maintaining a sustained concentration of levodopa in blood. It is a gastric retentive preparation for levodopa, characterized in that, the preparation contains a gastric resident layer showing a sufficient retentive property due to a high mechanical strength in the stomach and showing a good disintegrating property in an intestinal tract in addition to a drug releasing layer containing levodopa.
WO2014018671A1 Therapeutic compounds for the treatment of cancer The invention provides a compound of formula (I) wherein R1-R3 have any of the values defined in the specification, or a salt thereof. The compounds modulate the activity of the FGF1R pathway and are useful for treating cancer.
CN101518516B Sodium riboflavin phosphate lyophilized powder for injection and preparation method thereof The invention relates to sodium riboflavin phosphate lyophilized powder for injection and a preparation method thereof. The lyophilized powder for injection is prepared from following components in a The invention relates to sodium riboflavin phosphate lyophilized powder for injection and a preparation method thereof. The lyophilized powder for injection is prepared from following components in alyophilizing and drying way: 5-10g of sodium riboflavin phosphate (by lactoflavin), 20-40g of mannite, proper quantity of pH modifying agent and 1000-2000ml of water for injection. The sodium riboflavlyophilizing and drying way: 5-10g of sodium riboflavin phosphate (by lactoflavin), 20-40g of mannite, proper quantity of pH modifying agent and 1000-2000ml of water for injection. The sodium riboflavin phosphate lyophilized powder for injection is filled in an injection bottle made of amber low-borosilicate glass tube, has good stability and can be conveniently transported and stored, thereby proin phosphate lyophilized powder for injection is filled in an injection bottle made of amber low-borosilicate glass tube, has good stability and can be conveniently transported and stored, thereby proving more selections for clinical medication.ving more selections for clinical medication.
CN102078314A Medicament for treating cardiovascular disease and method preparing same The invention discloses a medicament for treating cardiovascular diseases and a method preparing the same. Trimethyl cyclopentadecanone or trimethyl cyclotridecanone or trimethyl cycloheptadecanone are respectively used for treating the cardiovascular diseases, or alternatively, one or more of cyclic ketones, pseudo-ginseng, salvia miltiorrhiza and borneol, according to a weight proportion of 1: (3-1): (1-3): (3-1), are made into oral liquid, pills, powder, paste or pellet. The invention further discloses a preparation method of the medicament.
US20120129933 Ceramide dimers and use thereof as pharmaceutical preparation or cosmetic preparation The invention relates to ceramide dimers which are constructed from two ceramide molecules which are crosslinked to each other via their lipophilic end. The ceramide molecules thereby have at least one hydrophilic group at their hydrophilic end for increasing the hydration shell of the dimer. The ceramide dimers according to the invention can be used as pharmaceutical preparation or as cosmetic preparation.
US20120004266 Dopamine-beta-hydroxylase genetic polymorphism and migraine The invention provides a method of determining whether or not an individual has a predisposition to migraine including the step of determining whether an isolated nucleic acid obtained from the individual comprises a nucleotide sequence corresponding to at least a fragment of a dopamine β-hydroxylase (DBH) gene promoter, wherein the presence of a −1021C→T single nucleotide polymorphism (SNP) in said nucleotide sequence indicates whether or not said individual has an increased predisposition to migraine compared to an individual without the polymorphism. DBH −1021C/C homozygotes are particularly susceptible to migraine. The −1021T allele may exert a protective effect. The method is particularly suited to detection of a predisposition to migraine with aura in females. The invention also provides a diagnostic kit for detecting a −1021C→T SNP associated with migraine. The method and kit may facilitate selection of individuals for migraine therapy which targets the dopaminergic system.
CN101822833A Medicament compound containing theophylines and statins The invention relates to a medicament containing theophylines and statins. In the invention, the theophylines and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor form a compound to obtain excellent synergistic effect. The medicament compound greatly reduces the toxic and side effect of aminophylline when used alone, and the pharmacy security is improved.
US8623422 Combination treatment with strontium for the prophylaxis and/or treatment of cartilage and/or bone conditions A combination treatment, wherein a strontium-containing compound together with one or more active substances capable of reducing the incidence of bone fracture and/or increasing bone density and/or improving healing of fractured bone and/or improving bone quality are administered for use in the treatment and/or prophylaxis of cartilage and/or bone conditions.
CN102948429A Livin bacteria removing liquid for marine organism The invention relates to a livin bacteria removing liquid for a marine organism. Effective sterilization components comprise marine organism alpha-spiral bactericidal peptide, seaweed polysaccharide derivatives, bio-enzyme and beta-chitosan quaternization hyaluronic acid derivants, and are prepared by a special process, so that the livin bacteria removing liquid is suitable for being used in restaurants, hotels, hospitals, shopping malls, banks, schools, kindergartens, homes, offices and journey, can be used as an after-wash remedial measure in hospitals, care centers, nursery centers, noshery, kitchens and bathtubs, or is used for sterilization of skin wounds, vulva cleaning and the like; and in addition, the removing liquid is wide in using range, is suitable for sterilizing skins of various field staffs, can effectively control propagation of typhoid fevers, flus, dysentery, pinkeye, gonorrhoea and various kinds of skin diseases, is long in sterilization and bacteriostat time and free of toxin and side effects, and has an efficiency of moisturizing the skins.
WO2010009535A1 A method for inhibiting poxvirus infection and pathogenesis using the alkaloid berberine Described herein is the use of the plant alkaloid berberine to inhibit orthopoxviruses,leporipoxvirus and yatapoxviruses. Inhibition is dose-dependent and occurs at concentrations in which host eel) toxicity is not observed.
EP2049136A1 Mitochondria-targeted antioxidants The present invention relates to a pharmaceutical or veterinary or nutritional or personal care composition comprising coenzyme Q10 (CoQI0), reduced CoQ1O, or mixtures thereof and oxygenated dibenzo-α-pyrone or an amino acyl ester thereof. The composition of the present invention is able to support and/or provide therapy to individuals at risk and/or under treatment for dysfunctions of energy metabolism, and specifically, for mitochondrial diseases.
WO2009010824A1 Dihydrochromenopyrazole derivatives as vanilloid receptor ligands The present invention relates to VR1 receptor ligands of the formula (I); and pharmaceutically acceptable salts, solvates, esters, stereoisomers, prodrugs, and N-oxides thereof. The present invention also relates to methods of treating diseases, conditions and/or disorders modulated by vanilloid receptors with these compounds, and processes for preparing them.
US20100278897 Intraocular bioactive agent delivery system with molecular partitioning system The present disclosure generally provides intraocular implants including at least one therapeutic bioactive agent and a molecular partitioning system. The molecular partitioning system comprises at least two phases wherein the first phase has an inherent viscosity equal or greater than the inherent viscosity of a second phase. The molecular partitioning system allows the intraocular implants to controllably release the at least one therapeutic bioactive agent into the surrounding tissues once implanted.
CN103462920A Oral cyclo-oxygenase-2 inhibitor Celecoxib composition The invention relates to a cyclo-oxygenase-2 inhibitor Celecoxib composition consisting of a quick-release part and a sustained-release part. The quick-release part comprises a medicine, a quick release material, a binder and a lubricant with effect of suppression of crystal; and the sustained-release part comprises the medicine, a slow-release material with effect of suppression of crystal, an adhesive and a lubricant. The preparation prepared by the invention has characteristics of simple preparation process, low energy consumption, fast onset, long maintenance time of blood drug concentration and stable concentration.
CN102764246A Trospium chloride controlled release capsule and preparation method thereof The present invention provides a trospium chloride controlled release capsule and a preparation method thereof. A capsule shell is filled with pills; the pills are wrapped with film coatings; a pill cladded with the coating is provided with a hole with a diameter of 0.05 mm; the pills in the capsule shell comprise an active ingredient trospium chloride; controlled release carriers in the pills are sodium carboxymethyl cellulose and natural alginate; a weight ratio of trospium chloride and the controlled release carrier is 1:0.6; a weight ratio of sodium carboxymethyl cellulose sodium and natural alginate is 1:0.8; viscosity of the sodium carboxymethyl cellulose is 3000-5000 centipoise; and viscosity of the natural alginate is 300-500 centipoise. According to the invention, the trospium chloride can be released at a constant speed in 9-12 h, so as to reduce frequency of drug usage.
US20110189274 Stable Pharmaceutical Compositions Of Montelukast Or Its Salts Or Solvates Or Hydrates A stable pharmaceutical composition includes a therapeutically effective amount of montelukast or its pharmaceutically acceptable salts, solvates or hydrates and a blend which includes microcrystalline cellulose and a flavoring agent and wherein said composition is substantially free of montelukast sulfoxide degradation product. A process for preparing such composition is also disclosed.
CN1583728A Compound extracted from eucalyptus plant and use thereof This invention provides a new method to purification 3 cycle sesquiterpene and the related compound contains the radical from eucalyptus. This compound has many application in treatment of tumours. Through in vivo and in vitro experiment in experiment animal, the sesquiterpene can inhbit many cancer cell include liver cancer, gastric carcinoma, esophageal carcinoma, prostatic csarcinoma, renal carcinoma and colon cancer, also it can inhibit the growth of the tumour that transplanted artificially in mouse.
CN101744971A Beautifying and beverage removing combined liquid and preparation method thereof The invention discloses a beautifying and beverage removing combined liquid and a preparation method thereof. The beautifying and beverage removing combined liquid is prepared from the following raw materials: saffron crocus, muskone, sage powder, pearl powder, radix paeoniae alba, aloe and nopal. The beautifying and beverage removing combined liquid prepared with the invention has obvious effects on freckles, acnes, blackheads, chloasma, withered and yellow black face, age pigments and sunburns, the total effective rate can reach more than 98%, and skin becomes white and tender and is rich in elasticity. Meanwhile, the invention has certain curing effect on acnes.
WO2011069063A3 Multicyclic compounds and methods of use thereof Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
CN101007139A An external applied medicine for treating burn and scald The invention discloses an externally-used medicament for treating burns and scalds, wherein the formulation of the medicament includes bletilla striata, gypsum fibrosum preparata, garden burnet root, rhubarb horsetails, dragon's blood resin, elephant skin, arborvitae tops, boneol, notoginseng, musk, bee wax and lard oil.
WO2009141412A1 1,6-disubstituted 3-azabicyclo [3.1.0] hexane derivatives for use as triple reuptake inhibitors The invention relates to compounds of formula (I), pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
EP1806149A1 Solid medicinal preparation improved in solubility and stability and process for producing the same The present invention relates to a solid formulation with improved solubility and maintained stability including a chemical substance poorly soluble in water as a pharmaceutically active ingredient formulated in an improved manner. More specifically, the present invention relates to a solid formulation having improved water-solubility which comprises a chemical substance poorly soluble in water as a pharmaceutically active ingredient, a water-soluble polymer substance and an inorganic porous substance, characterized in that (1) the chemical substance poorly soluble in water forms a solid dispersion together with the water-soluble polymer substance, (2) the water-soluble polymer substance forming the solid dispersion is in the form of fine pieces, and (3) the water-soluble polymer substance is in the form of fine pieces is maintained to be adsorbed on and/or adhered to the surface of the inorganic porous substance. The solid formulation can be produced by stirring and mixing a solution obtained by dissolving a chemical substance poorly soluble in water as a pharmaceutically active ingredient and a water-soluble polymer substance in an organic solvent with an inorganic porous substance and then granulating and drying the mixture.
CN1736380A Drug addiction-stopping formulation and preparation thereof The invention relates to a drug rehabilitation preparation and method for preparation, wherein the preparation comprises predetermined amount of tetrodontoxin monomer as the main effective composition, right amount of auxiliary material carrier, function modifier and tetrodontoxin derivative as the stabilizer, the acidic dissolvent carrier is selected from acetic acid / sodium acetate, or citric acid / sodium citrate, or citric acid / disodium hydrogen phosphate, the function modifier is at least one selected from trichlorbutanolum, benzoic alcohol and lignocaine hydrochloride.
WO2010102991A3 Riluzole liquid emulsions Physically and chemically stable liquid O/W and W/O emulsions of riluzole are disclosed, together with methods for the preparation thereof. Such emulsions contain riluzole or a pharmaceutically acceptable salt or derivative thereof in amounts from about 0.1 % to about 20 % w/w, preferably from about 0.5% to about 5% w/w; such emulsions are devoid of the known local (mouth) anaesthetic effects of riluzole.
US8614210 Process for preparing pharmaceutical ophthalmic compositions Pharmaceutical ophthalmic compositions comprising active ingredient(s) such as carbonic anhydrase inhibitor (CAI) or combinations and processes for making such compositions and the use of these compositions in patient populations including pediatric populations. A process for preparing an ophthalmic composition comprising a carbonic anhydrase inhibitor, which comprises a) preparing a slurry comprising a carbonic anhydrase inhibitor and a surfactant; b) preparing a polymer slurry comprising a polymer and water; c) preparing a solution comprising tonicity and preservative agents; d) mixing the polymer slurry of step b and the solution of step c, to form a vehicle concentrate and adjusting pH; e) adding the slurry of step a, to the vehicle concentrate of step d and mixing to homogenize; f) autoclaving the mixture of step e; g) sizing the mixture of step f, under aseptic condition.
WO2010067617A1 Lipid membrane structure Disclosed is a lipid membrane structure for delivering a substance such as a pharmaceutically effective component or a nucleic acid to a target tissue or an organ (for example, the liver). The lipid membrane structure is in the form of a liposome surface-modified with an MPC polymer and GALA, or the like.
CN101559053A 5-membered heterocycle derivatives, production thereof and use thereof as medicaments The invention relates to compounds of general formula (I) which can be used for producing a medicament for inhibiting monoamine oxydases (MAO) and/or for lipidic peroxydation and/or for acting as modulators of sodium channels. The resulting medicament is particularly for use for treating Parkinson's disease, senile dementure, Alzheimer's disease, Huntington's chorea, amytrophic lateral sclerosis, schizophrenia, depression, psychosis, pain and epilepsy. The inventive compounds correspond to general formula (I), wherein Het is a 5-membered heterocycle comprising 2 heteroatoms and is such that general formula (I) corresponds exclusively to one of sub-formulae: (I)1, (I)2, (I)3 and (I)4, wherein A represents especially a substituted phenyl or biphenyl radical, B represents especially H or an alkyl radical, X represents especially NH or S, Y represents O or S, n is a whole number from 0 to 6, R and R represent, independently of each other, especially radicals chosen from the following: a hydrogen atom or an alkyl or cycloalkyl radical; and OMEGA represents NRR or OR, R and R representing especially radicals chosen from the following:; an atom of hydrogen and an alkyl, cycloalkyl, alkynyl, cyanoalkyl alkoxycarbonyl, aralkoxycarbonyl or (cycloalkyl)oxycarbonyl radical and R representing a hydrogen atom or an alkyl, alkynyl or cyanoylkynyl radical.
CN101926806A Application of 17 phosphorus estrogen compound in preparation of emergency contraception The invention relates to an application of a 17 phosphorus estrogen compound in the preparation of an emergency contraception, provides an application of a compound shown in formula (II) in the preparation of an emergency contraception and also provides an emergency contraception. The emergency contraception is characterized by comprising the compound shown in formula (II) and a pharmaceutically acceptable vector, wherein the dosage of the compound shown in formula (II) is 1-100mg.
CN1596899A Dexamehasone palmitate freeze-dried emulsion and its preparation method A freeze-dried emulsion of dexamethasone palmitate contains dexamethasone palmitate, oil phase, emulsifier, stabilizer, pH regulator and freeze-drying protector.
CN103601670A Piplartine analogue, and preparation method and application thereof The invention relates to the technical field of medicines. Piplartine is alkaloid extracted from perennial herbaceous vine piper longum of piperaceae. The invention provides a Piplartine analogue, which comprises a cis-trans-isomer, and any arbitrary mixture in those forms or medicinal salt thereof, and the structural formula of the Piplartine is shown in a general formula (I). The invention also provides a preparation method of substituted Piplartine compounds, and an application thereof in preparation of an antitumor medicament.
CN103463048A Application of Lycojaponicumin A in medicaments for promoting small intestine peristalsis The invention relates to application of Lycojaponicumin A in preparation of medicaments for promoting small intestine peristalsis. According to pharmacological experiments, the Lycojaponicumin A has a good effect of promoting small intestine peristalsis. The application of the Lycojaponicumin A in preparation of the medicaments for promoting small intestine peristalsis is made public for the first time; the skeleton type is completely novel and the Incarviatone A has an unexpectedly strong small intestine peristalsis promoting activity, so the probability that other compounds give any revelation does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently made in preparation of the medicaments for promoting small intestine peristalsis.
US20120301393 Modified ubiquitin proteins having a specific binding activity for the extradomain b of fibronectin The present invention refers to novel recombinant proteins obtained from modified ubiquitin capable of binding the extradomain B of fibronectin (ED-B). Furthermore, the invention refers to fusion proteins comprising said recombinant protein fused to a pharmaceutically and/or diagnostically active component.
US7576086 N1-benzyl-N4-(phenylpropane-2-yl-3-ol)piperazine; triple action on hydroxytryptamine (5-HT), noradrenalin (NA)and dopamine(DA); on brain synapses; cytochrome P-450 monooxygenase enzyme system antagonists; enzyme inhibitors; side effect reduction Aryl alkanol piperazine derivatives of the formula and pharmaceutical compositions comprising the same. Also disclosed are methods for treating depression using the pharmaceutical composition. Compounds of the invention have excellent dual inhibitory actions to the uptake of the mono-amines neurotransmitter, good antidepressant activities and minor side effects.
CN101869585A Composition for assisting treatment effect of hepatitis B medicament The invention provides a composition for assisting treatment effect of a hepatitis B medicament, which comprises spirulina. The content of a zinc element contained in the spirulina is between 1,000 and 1,500 ppm, the content of a selenium element is between 34 and 42 ppm, and the content of a chromium element is between 30 and 40 ppm. The aim of assisting the treatment of the hepatitis B medicament is fulfilled by supplementing trace elements.
WO2008008660A3 Cyclopentane derivatives as antiglaucoma agents Disclosed and described herein are compounds of the formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed and described.
EP1978962A2 Compositions and methods of treatment using modulators of motonueron diseases The invention disclosed herein describes a novel therapeutic target for motoneuron diseases (altered dynamics of microtubules in neurons); a method for measuring the state of activity of this therapeutic target in subjects with established, incipient, or potential motoneuron disease; the discovery of drug agents that modulate neuronal microtubule dynamics in living subjects with motoneuron diseases; the discovery that administration of such agents, alone or in combinations, can provide marked neuroprotective therapy for living subjects with motoneuron diseases including delay in symptoms and prolongation of survival; and the discovery that monitoring of neuronal microtubule dynamics in subjects with motoneuron diseases, in response to therapeutic interventions, allows diagnostic monitoring for optimization of therapeutic regimen and strategy for individual subjects or for drug trials.
US8343979 Use of alkanoyl L-carnitine for the treatment of erectile dysfunction Erectile dysfunction is treated with a combination of propionyl L-carnitine in combination with sildenafil, apomorphine prostaglandin El, pentolamine and papaverine.
US20080262031 4-Aminoquinoline Derivatives as Antimalarials New 4-aminoquinoline derivatives having the general formula (I) wherein R, M, X, Y and T have the meaning described in the specification, as potent antimalarials active also on chloroquine-resistant Plasmodium falciparum malaria strains.
CN102827069A Method for preparing two organic compounds by using chlorogenic acid as raw material and application thereof The invention discloses a method for preparing two organic compounds by using chlorogenic acid as a raw material and an application thereof. The two organic compounds are an organic compound which is formed by chlorogenic acid (HAC) and 2,2'-bipy and has a chemical name of (CA).( 2,2'-Hbipy), and an organic compound which is formed by chlorogenic acid and 1,10-phen and has a chemical name of (CA).( 1,10-Hphen). Through tests, the organic compound (CA).( 2,2'-Hbipy) formed by chlorogenic acid and 2,2'-bipy has good bacteriostatic effect on staphylococcus aureus, escherichia coli, pseudomonas aeruginosa, and candida albicans; the organic compound (CA).( 1,10-Hphen) formed by chlorogenic acid and phen has good bacteriostatic effect on staphylococcus aureus and salmonella; the organic compounds of the invention are antibacterial agents which are applicable to industry such as food and medicine, and can be used for preparing food and medicine products with bacteriostatic effect.
WO2013188396A1 Combination of therapeutic agents for treating hcv infection Embodiments disclosed in the present application relate to a composition that can include a hepatitis C viral nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof, a hepatitis C viral protease inhibitor, or pharmaceutically acceptable salt or prodrug thereof, and a hepatitis C viral non-nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof. Additional embodiments disclosed relate to methods for treating a disease condition such as a hepatitis C virus infection, liver fibrosis and/or impaired liver function with a hepatitis C viral nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof, a hepatitis C viral protease inhibitor, or pharmaceutically acceptable salt or prodrug thereof, and a hepatitis C viral non-nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof.
WO2012107706A1 Phenothiazine diaminium salts and their use The invention relates to compounds of general formula (I): wherein: each of R1 and R9 is independently selected from: -H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: -H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: -H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; and wherein: each of RA and RB is independently selected from: C1-4alkyl, halogenated C1-4alkyl, and C6-10aryl; or RA and RB are linked to form a group selected from: C1-6 alkylene and C6-10 arylene; and pharmaceutically acceptable salts thereof, which are useful in the treatment of, for example, Alzheimer's disease. In other aspects the invention also relates to novel formulations of 3,7-diamino-10H-phenothiazinium salts.
US8247415 Hydroxymethyl pyrrolidines as β3 adrenergic receptor agonists The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.
CA2175375C Glucosamine disaccharides, method for their preparation, pharmaceutical composition comprising same, and their use The invention relates to .beta.(16) glucosamine disaccharides having general formula (I) to a method for preparing these disaccharides, comprising the steps of: i) providing a starting material comprising lipid A moiety of lipopolysaccharide-comprising microorganisms; and ii) subjecting the starting material to an alkaline treatment such that lipid A moiety is O-deacylated at the 3-position and at the 3'-position, to pharmaceutical compositions comprising as an active ingredient these disaccharides, and to these disaccharides for use as an immunomodulating agent, anti-tumor agent, and vaccine component.
CN1857356A Preparation and application of total seabuckthorn flavone composition The present invention relates to compound preparation with total seabuckthorn flavone composition as main component for treating cardiac and cerebral vascular diseases. The total seabuckthorn flavone composition contains total seabuckthorn flavone in 1-99 wt% and total sowthistle-leafixeris flavone in 1-99 wt%, and is compounded with pharmaceutically acceptable supplementary material to prepare various kinds of preparation. The medicine of the present invention is used in preventing and treating cardiac and cerebral vascular diseases, senile dementia, and other diseases.
CN102875549A 7-arylamine/methylamino-5-amino-6-azaindole derivative, preparation method and application The invention provides a 7-arylamine/methylamino-5-amino-6-azaindole derivative, and medicinal salt thereof. The derivative is prepared by reacting aminomethyl aromatic heterocyclic with 2,6-dichloro-3-nitropyridine, and reacting a reaction product with di-tert-butyl dicarbonate in a tetrahydrofuran solution under the protection of Boc at room temperature for 9 hours by taking dimethylamino pyridine as a catalyst. Raw materials required during synthesis are readily available, the derivative and the medicinal salt thereof are convenient to prepare and suitable for industrial production. Pharmacological experiments prove that the derivative and the medicinal salt thereof have relatively good in-vitro inhibitory and proliferous effects on a plurality of tumor cell strains such as human colon cancer cells, human leukemia cells, human lung cancer cells and human ovarian cells, the relatively good in-vitro cytostatic action and preliminary enzyme inhibitory activity are generally shown, and the derivative can be applied to preparation of antitumor medicines. The derivative is shown in the following general structural formula.
CN101618021B Chitosan coating medicine slow release microsphere and preparation method thereof The invention discloses a chitosan coating medicine slow release microsphere and a preparation method thereof. The chitosan coating medicine slow release microsphere comprises a condensate capsule shell of chitosan and glutaric dialdehyde, core medicine resveratrol, oxidative resveratrol, pterostilbene or white cedar alcohol, wherein the core medicine resveratrol, the oxidative resveratrol, the pterostilbene or the white cedar alcohol are coated into the capsule shell. The preparation method is simple and easy, the preparation cost is low, the microsphere envelop rate is 10-50 percent, the microsphere is round and has good dispersivity, the stability of the original medicine is increased, and the chitosan coating medicine slow release microsphere realizes the function of medicine slow control and release and can be conveniently matched with other medicines. The chitosan coating medicine slow release microsphere is suitable for preparing a slow release formulation of medical resveratrol, oxidative resveratrol, pterostilbene and white cedar alcohol.
WO2013184029A1 Solid dosage form having expectorant, local coating, and anti-inflammatory effects (variants) The invention relates to the pharmaceutical industry and the field of medicine and can be used in the creation and administration of solid dosage forms having expectorant, local coating, and anti-inflammatory effects. The aim of the present invention is to create an effective solid dosage form based on an extract of the herb Althea officinalis, having expectorant, local coating, and anti-inflammatory effects, by means of using the mineral substances potassium, magnesium, iron, manganese, zinc, copper, and also isotopes of carbon-13. The technical results of the invention are a more rapid onset of therapeutic effect, an enhanced therapeutic effect with no increase in the concentration of Althea officinalis extract, and improved stability for the duration of the shelf life.
CA2592158A1 Methods of modulating the activities of alpha7 nicotinic acetylcholine receptor The present invention provides methods for identifying compounds useful in modulating a7 nicotinic acetylcholine receptors. The invention also provides compounds that prevent, suppress or inhibit desensitization of an a7 nicotinic acetylcholine receptor, and which resensitize such receptors. Pharmaceutical compositions, and methods of treatment, particularly in regard of neurological diseases are also described.
EP2046289B1 Compositions and kits of phenylephrine The invention relates to a clear device: comprising a composition contained in a device; wherein said composition comprising a pharmaceutical active selected from the group consisting of phenylephrine, its free and addition salt forms, and mixtures thereof. Also disclosed are kits comprising: a composition contained in a device; wherein said composition comprising a pharmaceutical active selected from the group consisting of phenylephrine, its free and addition salt forms, and mixtures thereof.
US20050250793 Preventives/remedies for hot flash It is intended to provide a preventing or treating agent for hot flash which comprises a nonpeptidic compound having gonadotropin releasing hormone antagonistic activity, in particular, a preventing or treating agent for hot flash which comprises a nonpeptidic compound having gonadotropin releasing hormone antagonistic activity, wherein said compound is capable of entering the brain.
US20120202855 Methods for treating hyperlipidemia with intermediate release nicotinic acid compositions having unique biopharmaceutical characteristics Methods for treating hyperlipidemia with intermediate release nicotinic acid formulations having unique biopharmaceutical characteristics, without causing drug-induced hepatotoxicity to a level which would require discontinuation of the therapy, are disclosed. According to the methods of the present invention, the intermediate nicotinic acid formulations are administered as a single dose once-a-day during the evening or at night. While the methods of the present invention contemplate administering the intermediate release nicotinic acid formulations at any time during a 24 hour period, it is preferable to administer them as a single dose during the evening or at night between about 6:00 pm. and 12:00 a.m., preferably between about 8:00 p.m. and 12:00 a.m., and most preferably between about 8:00 p.m. and 10:00 p.m.
US7528140 Substituted pyrrolo[3,2-d]pyrimidines as glycogen synthase kinase (GSK) inhibitors The invention provides pyrrolo[3,2-d]pyrimidine derivatives represented by formula (I), and their medically acceptable salts. The compounds of the invention exhibit GSK-3 inhibiting activity and are therefore expected to be useful as therapeutic or prophylactic agents for conditions in which GSK-3 is implicated, such as diabetes, diabetes complications, Alzheimer's disease, neurodegenerative diseases, manic depression, traumatic encephalopathy, alopecia, inflammatory diseases, cancer and immune deficiency.
WO2007100536A1 DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE The present invention provides a 10,11-dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol]-5'(1'H)-one compound of formula (I). Also provided are methods and compositions for the inhibition of ß-secretase (BACE) and the treatment of ß-amyloid deposits and neurofibrillary tangles.
CN101361804B Enteral nutrition emulsion for tumor patient The invention relates to an enteral nutrition emulsion used for tumor patients, which is characterized in that the emulsion of every 1000mL contains 30g to 50g of holothurian amylase, abalone amylase, oyster amylase or meretrix amylase, 50g to 70g of pearl oyster meat powder, soybean protein powder or fish protein powder, 15g to 25g of spirulina powder, 6ml to 8 ml of olive oil, 3g to 8g of an emulsifier and water of rest amount. The enteral nutrition emulsion can improve the activity of free radical scavenger enzymes of the organism, enhance the oxidation resistance of tissues and adjust theimmune function so as to ensure the increasing trends of the weight, the upper-arm circumference and the skin fold thickness of the brachial triceps muscle of a sufferer, and gradually normalize various blood biochemical indicators, thereby reducing damages caused by operation or radiotherapy and chemotherapy to the immune system, being capable of providing nutritional supports for the tumor patients of head and neck cancer, esophageal cancer, pancreatic cancer, liver cancer, and the like as well as the tumor patients who accept radiotherapy and chemotherapy, and promoting the recovery of thepatients.
US20120058100 Modulation of drug release rate from electrospun fibers Disclosed are co-electrospun polymeric fibers comprising polymers comprising pharmaceutically active agents and/or biologically active agents and capable of release at a combined release rate. Also disclosed are processes for preparing polymeric fibers capable of release at a combined release rate. Also disclosed are processes of modulating delivery rate of pharmaceutically active agents and/or biologically active agents. Also disclosed are processes of delivering pharmaceutically active agents and/or biologically active agents. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
US7332586 Active agent and a nuclear localization signal and methods of modulating gene expression and protein expression employing the nanoparticle delivery vehicle. A representative method includes providing a nanoparticle delivery vehicle comprising A nanoparticle delivery vehicle, comprising a nanoparticle, an active agent and a nuclear localization signal and methods of modulating gene expression and protein expression employing the nanoparticle delivery vehicle. A representative method includes providing a nanoparticle delivery vehicle comprising a nanoparticle having a diameter of about 30 nm or less, an active agent and a nuclear localization signal; and contacting a target cell with the nanoparticle delivery vehicle, whereby an active agent is delivered to the nucleus of a target cell. Another representative method includes providing a nanoparticle delivery vehicle comprising a nanoparticle having a diameter greater than or equal to about 30 nm, an active agent and a nuclear localization signal; and contacting a target cell with the nanoparticle delivery vehicle, whereby an active agent is delivered to the cytoplasm of a cell.
US20090247483 Method for Treatment of Macular Degeneration Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by elevating cAMP by administering or stimulating receptors coupled to a Gs protein in an amount sufficient to decrease the elevated pHL or restore acidity of said lysosomes, specifically by administering or stimulating receptors comprising D1-like dopamine receptors by the use of D1-like dopamine receptor agonists. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.
US20110269706 Hydroxamic Acid Derivatives The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
WO2013013195A1 Compositions and methods for treating polycythemia vera and essential thrombocythemia Provided herein are compositions and methods for treating polycythemia vera (PV) and/or essential thrombocythemia (ET) in a subject. The methods comprise administering to the subject an effective amount of compound which is which is N-ieri-butyl-3-[(5-methyl-2- { [4-(2-pyrrolidin-l-ylethoxy)phenyl] amino }pyrimidin-4-yl)amino]benzenesulfonamide or a pharmaceutically acceptable salt or a hydrate thereof.
US20070280939 Prostatic Acid Phosphatase Antigens The invention relates to peptides from Prostatic Acid Phosphatase (PAP), especially those identified as PAP.135 and PAP.161. The nucleic acid molecules encoding the peptides, antibodies against the peptides, and the use of such peptides, nucleic acids and antibodies in immunotherapy, vaccines and assays are also included in the scope of the invention.
CA2594270A1 Antimicrobial hand wash An antimicrobial hand wash includes a soap, an antimicrobial agent, and an amine salt. The amine salt is found to increase the antimicrobial efficacy of the hand wash. The amine salt produced through the reaction of monoethanolamine and lactic acid is of particular interest as a soap addition. In processes of this invention, it is possible to create the desired amine salt in the soap in situ.
US20080234217 Double stranded nucleotide sequences for use as tools in tissue targeted gene expression inhibition and treatment of cancer, vascular, neuronal and endocrine diseases The present invention provides methods and compositions for attenuating expression of a target gene in vivo. In general, the method includes administering RNAi constructs (such as small-interfering RNAs (i.e., siRNAs) that are targeted to particular mRNA sequences, or nucleic acid material that can produce siRNAs in a cell), in an amount sufficient to attenuate expression of a target gene by an RNA interference mechanism. In particular, the RNAi constructs may include one or more modifications to improve serum stability, cellular uptake and/or to avoid non-specific effect. In certain embodiments, the RNAi constructs contain an aptamer portion. The aptamer may bind to human serum albumin to improve serum half life. The aptamer may also bind to a cell surface protein that improves uptake of the construct.
EP1910367A2 Pyrimidine or triazine fused bicyclic metalloprotease inhibitors The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 inhibitors.
CN1657071A Asarum brain injection and its preparation method An injection of asarone for treating epilepsy, cough, asthma, etc is prepared from grass-leaved sweetflag rhizome through extracting the volatile component (beta-asarone).
EP2311446A1 Compositions comprising Tramadol and Celecoxib in the treatment of pain The present invention relates to pharmaceutical compositions comprising tramadol and celecoxib and their uses as medicaments or analgesics, more particularly for the treatment of severe to moderate pain with an inflammation component.
US20070191291 Compound antibacterial drugs comprising n-acetyl-d-glucosamine The use of the combination of N-acetyl-D-glucosamine and antibiotics for the preparation of antibacterial drugs is disclosed. In the therapies of infections with antibiotics, the pathogens may be changed into slender shaped forms called cryptic growth cells (CGCs), CGCs can colonize and thereby physiological drug resistance arises. In the meantime, normal bacteria colonies in the body may be also changed into CGCs upon administration of antibiotics. These changes result in complications after the therapies, such as disorder of bacteria colonies in the body, disorder of GI functions and other chronic diseases. The combination of antibiotics and N-acetyl-D-aminoglycosamine can prevent of CGC, and the complications after antibiotics therapy.
CN103751191A Combination medicine for treating psoriasis The invention relates to a combination medicine for treating psoriasis, which comprises the following components: 5 mg of methotrexate, 80 mg of silymarin, 15 mg of vitamin B4, and 20 mg of famotidine; the medicine is a four-layer capsule; famotidine is filled between the first capsule layer and the second capsule layer; methotrexate is filled between the second capsule layer and the third capsule layer; silymarin is filled between the third capsule layer and the fourth capsule layer; vitamin B4 is filled in the fourth capsule layer; the thick of the first capsule layer is 1 mm; the thick of the second capsule layer is 1 mm; the thick of the third capsule layer is 3 mm; the thick of the fourth capsule layer is 2 mm. The combination medicine for treating psoriasis not only can play a role of treating psoriasis but also can protect liver and stomach in the treating process; the number of leukocyte is kept in the normal level; due to arrangement of the multi-layer capsules, various medicines are independently separated; the practical drug delivery time is controlled; the maximum pharmaceutical effects of medicines are ensured.
CN101456797B Walnut powder with anticancer activity as well as preparation method and use thereof The invention discloses maraniol with anticancer activity and a preparation method and application thereof. The maraniol is a diaryl heptane compound; the molecular formula of the maraniol is C20H24O4; and the chemical formula is shown in (I). As proved by in vivo and in vitro pharmacological activity researches, the compound has strong anticancer activity, so that a novel anticancer medicine which takes the maraniol as a raw material can be hopefully developed.
CN101327233B Compound external-use formulation for treating gonorrhoea and nongonococcal urethritis The invention relates to a compound external preparation for treating gonorrhea and non-gonorrhea, which is prepared by five raw materials of acorn, cyrtomium rhizome, tetracycline, calcined soda and sodium dodecyl benzene sulphonate. The formulation of the preparation is well prepared, the preparation method is simple, and each drug exerts merit and cooperates to treat gonorrhea and non-gonorrhea synthetically. Compared with the prior art, the preparation can effectively deracinate sexual diseases such as gonorrhea, non-gonorrhea and the like caused by various infections such as male urethritis, prostatitis, female vaginitis, cervical erosion which are resulted from diplococcus gonorrhea, candidaalbicans, mycoplasma, chlamydia, infusorium, etc. The preparation has the advantages of fast efficacy, high healing rate, low recurrence rate, being convenient to carry and use, etc.
US20100298365 Topical administration carrier composition and therapeutic formulations comprising same A topical administration carrier composition including water, glycerin and polysorbate, suitable for use in formulations with active ingredient compositions containing active ingredients such as minoxidil that are susceptible to systemic penetration, and solvents that are susceptible to evaporative loss, when the active ingredient composition is topically applied to the body. The carrier formulation retards the evaporative losses of the solvent component(s) and systemic migration losses of the active ingredient composition, to provide sustained topical action, in relation to formulations lacking the carrier composition of the invention.
EP2600832A1 Combination of compounds for treating or preventing skin diseases The invention relates to a combination of compounds for treating skin diseases and particularly rosacea and ocular rosacea. It is the combination of a compound selected from azelaic acid and salts thereof with a compound of the alpha-1 or alpha-2 adrenergic receptor agonist family. The invention also relates to a product in the form of a kit containing: (a) a first composition comprising a compound selected from azelaic acid and salts thereof, and (b) a second composition different from the first one and comprising a compound of the alpha-1 or alpha-2 adrenergic receptor agonist family, as a combination product for application thereof as a medicament for treating and/or preventing skin diseases and in particular rosacea and ocular rosacea, wherein said first and second compositions can be applied simultaneously, separately or with a time delay.
US20110229456 Modulation of immunostimulatory properties of oligonucleotide-based compounds by optimal presentation of 5' ends The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers of the invention comprise at least two oligonucleotides linked at their 3′ ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunostimulatory oligonucleotide and having an accessible 5′ end.
US7414054 3-(arylamino)methylene-1, 3-dihydro-2H-indol-2-ones as kinase inhibitors The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
CN103379899A Pharmaceutical preparation containing selenite or selenite-containing compounds for treating cervical dysplasia or carcinomas The invention relates to compositions containing selenite-containing compounds and pharmaceutically acceptable acids, selected from citric acid, acetic acid, malic acid, carbonic acid, sulphuric acid, nitric acid, hydrochloric acid, fruit acids or mixtures thereof, for use for treating cervical inflammations, dysplasia and/or carcinomas.
EP1296982B1 1-(heteroaryl-phenyl)-condensed pyrazol derivatives as factor xa inhibitors The present application describes heteroaryl-phenyl heterobicycles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
US20100197626 Biomarkers for Depression and Methods Using the Same The present invention provides various biomarkers of depression. The present invention also provides various methods of using the biomarkers, including methods for diagnosis of depression, methods of determining predisposition to depression, methods of monitoring progression/regression of depression, methods of assessing efficacy of compositions for treating depression, methods of screening compositions for activity in modulating biomarkers of depression, methods of treating depression, as well as other methods based on biomarkers of depression.
US20100035811 Phosphoinositide Modulation For The Treatment Of Neurodegenerative Diseases The present invention relates to the use of agents that inhibit the toxic effects of amyloid oligomers by increasing intracellular levels of phosphoinositol 4-phosphate (PI(4)P, or “PIP”) and/or phosphotidylinositol 4,5-biphosphate (PI(4,5)P2 or “PIP2”), the use of such agents for the treatment of neurodegenerative diseases, methods of treating neurodegenerative diseases by administration of agents which alter lipid metabolism, and methods of identifying agents which alter the association of presenilins with γ-secretase and lipid rafts.
CN101011357A Process for preparing Paclitaxel liposome preparation The invention relates to a method for preparing drug rehabilitation liposome agent, which comprises that using film disperse method or atomizing drying method to prepare long-circulation rehabilitation liposome, using cholesterol, distearin acyl phosphatidyl choline and myristate as stabilizers, using sucrose as freezing preservative, using chloroform and chloroform as organic solvents; and using amphipathic carbowax derivative to decorate the liposome membrane; and using compression or high-pressure homogeneity method to make the diameter of liposome smaller than 100nm and the package rate higher than 85%. The invention has less toxicity and high stability, as one novel drug slow-release target agent.
US6972179 RRP sequences and knockout mice and uses thereof RRP genes are identified as modulators of the p53 or p21 pathway, and thus are therapeutic targets for disorders associated with defective p53 or p21 function. Methods for identifying modulators of p53 or p21, comprising screening for agents that modulate the activity of RRP are provided. Modulating agents identified using the methods of the invention can be used to specifically inhibit growth of tumor cells that overexpress an RRP protein. mRRP1 knockout mice are also provided.
CN102391262A Antimicrobial compound containing 3-carboxyalkyl rhodanine derivative The invention provides a novel compound containing a 3-carboxyalkyl rhodanine structure and a synthetic method thereof. The novel compound has a wide antimicrobial spectrum, shows remarkable antibiotic activity on Gram-positive bacteria, and has a better bacteriostatic effect than common clinical norfloxacin, so that the compound has the potential of being prepared into an antimicrobial medicament. A lead compound is provided for the research of a new antimicrobial medicament. The synthetic method of the compound is simple and reasonable, and has low production cost.
US8734830 Manufacturing method and apparatus of ultrafine particles having uniform particle size distribution The present invention relates to a novel technology for forming fine particles with a size of 0.0˜23 microns from a solid that can be dissolved in a liquid solvent and is not decomposed by heat. The particle preparation technology according to the present invention may be applicable to the fields of food, cosmetics, biopolymer, polymer compositions, and pharmaceuticals.
CN101011460A Pharmaceutical composition with both depigmenting and whitening effects The invention discloses a pharmaceutical composition having beauty treatment effect for treating acne, which comprises dahurian angelica root, licorice root, astragalus root and/or arbutin extract. The composition has good effect in desalination and removal of color stains.
US20100048534 Crystalline lestaurtinib hydrates and crystalline lestaurtinib hemihydrate hemiacetonitrileate and crystalline lestaurtinib hemihydrate hemitetrahydrofuranate Crystalline lestaurtinib hydrates and crystalline lestaurtinib hemihydrate hemicetonitrileate and crystalline lestaurtinib hemihydrate hemitetrahydrofuranate, processes to reproducibly make them and methods of treating patients using them are disclosed.
CN103120673A Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor The invention provides an application of Aphanamixoid A to the preparation of a monoamine oxidase (MAO) inhibitor. Compared with the existing MAO inhibitor, the MAO inhibitor provided by the invention is greatly improved on the aspects of inhibitory activity and selectivity to MAO-A and MAO-B. The application of the Aphanamixoid A to the preparation of the MAO inhibitor, related by the invention, is disclosed for the first time; a framework type of the Aphanamixoid A is brand new, and Aphanamixoid A has unexpected strong inhibitory activity to MAO, so that no possibility that any revelation is given by other compounds exists, and Aphanamixoid A has remarkable substantive features and is also remarkably improved on the aspect of treating MAO imbalance related diseases.
US7361760 Substituted naphthyridine derivatives as inhibitors of macrophage migration inhibitory factor and their use in the treatment of human diseases Inhibitors of MIF having a naphthyridine backbone are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R, R1, R2, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.
CN1969841A Herbal extract for treating rheumatoid arthritis The invention relates to the use of apple polyphenol in preparing medicaments or health products for the treatment and/or prevention of rheumathritis or rheumatoid arthritis pertaining to the field of pharmaceuticals or health products, wherein apple polyphenol obtained through industrialized production is used as the raw material. The pharmaceuticals and health products can be obtained through conventional preparing processes for for mass production at low cost.
EP1534241A1 Transdermal aerosol compositions The present invention provides a pharmaceutical composition for transdermal delivery comprising: one or more physiologically active agents; one or more dermal penetration enhancers; a pharmaceutically acceptable carrier comprising a volatile solvent; and a hydrofluorocarbon propellent; wherein the carrier and penetration enhancers combine to provide a single-phase solution of the one or more physiologically active agents.
CN1977941A Method for preparing female lotion fromaloe and its use The present invention relates to a medicine composition cleaning solution for bacteriostatic cleaning gynecopathy. It is made up by using 10-60 wt% of aloe, 0.01-0.2 wt% of benzalkonium bromide, 0.05-0.5 gram molecular concentration of boric acid buffer solution, 0.01-0.2 wt% of borneol and rest excipient through a certain preparation method.
CN1884261A Hydantion method compolete preparation of chromium selenomethionine compounds (III) and its uses The invention relates to a integrated method for preparing seleno chromium methionine (III) through hrdantoin and its application. The intermediate seleno acimetion with multiple biological activity and usage can be prepared with said method. The Cr3+ in chromium trichloride hexahydrate can produce three modifications of different construction with one to three acid molecules, which are named as I-seleno chromium methionine, II-seleno chromium methionine and seleno chromium methionine (containing three acid molecules). The difference in performance and effect of three modifications is favorable for controlling content and proportion of selenium and chromium in compound. The compound can be widely used in medicine, health care product, feed addictive and cosmetics, especially used to produce capsule, tablet and oral liquid prevent and treating diabetes.
CN101367861A 2-hydroxyl-3-deoxidized pentacyclic triterpenoid and derivant, preparation method and uses thereof The present invention relates to the field of medicines, in particular to a pentacyclic triterpene compound with a series of formula (I) or (II) and a preparation method and applications in the preparation of medicines used to prevent and treat diabetes, angiocardiopathy, cerebrovascular disease and tumors thereof. The definition of R1-8 can be seen in the description.
CN103251634A Fosfomycin sodium/sulbactam sodium injection The invention discloses a fosfomycin sodium/sulbactam sodium injection. A pathogenic bacteria drug resistance monitoring network of the ministry of health displays that the drug resistance rate of bacteria is increased gradually recently, and especially, the drum resistance rate of non-fermented fungus in gram-negative bacillus exceeds 50 percent. The increase of the drug resistance of the bacteria is a worldwide difficulty, and a new antibacterial is researched and developed by more than 10 years, so that the speed is remarkably lags behind the increase speed of the drug resistance of the bacteria. The fosfomycin sodium/sulbactam sodium injection is a compound preparation, and has a broad-spectrum antibacterial activity; laboratories and clinical research results indicate that the fosfomycin sodium/sulbactam sodium injection has obvious antibacterial activity to the drug-resistant gram-negative bacillus as an existing antibiotic, and has the laboratory sensibility reaching 100 percent, and clinical bacteria removal rate reaching 95 percent; and a compound preparation in a solution state is stable in physicochemical properties. The compound preparation is simple in production process, is easily transformed into a product, can be produced by any one qualified pharmaceutical enterprise, and is extremely high in expected social benefit and economic benefit.
CN103333134A 2-(3-cyano-4-alkoxy) phenyl-4-substituted thiazole-5-formic acid compound, composition as well as preparation methods and applications thereof The invention relates to a 2-(3-cyano-4-alkoxy) phenyl-4-substituted thiazole-5-formic acid compound which has xanthine oxidase inhibitory activity and is shown in a general formula I, a composition and preparation methods thereof. The invention also relates to applications of the compound and the composition thereof to preparation of medicaments for treating and/or preventing hyperuricemia and gout diseases. In the formula I, R2 is substituted or unsubstituted phenyl or a substituted or unsubstituted heteroaromatic radical, R1 is a substitutive aliphatic group of a straight chain or a branched chain, substituted or unsubstituted alicyclic hydrocarbonyl or substituted or unsubstituted aryl alkyl and A is an oxygen atom, a sulfur atom or a nitrogen atom.
WO2013022369A1 Complex zinc and alpha-chlorocarboxylic acid compounds for treating skin lesions The invention relates to the field of medicine, and specifically to preparations for treating skin lesions, in particular viral, benign, precancerous and cancerous, non-metastasizing, dysplastic and inflammatory lesions of the visible mucous membranes, and also viral and fungal skin and nail lesions, and for correcting wrinkles and senile pigment blemishes, said preparations comprising solutions of complex compounds of salts of zinc and alpha-chlorocarboxylic acids of general formula [Zn(RCH2-xClxCOOH)n (Н2O)4-n]+2 *2 [RCH2-x ClxСОО]-, where R = alkyl, Н or Cl, х = 1-2 and n = 0-4, in a corresponding alpha-chlorocarboxylic acid, wherein the content of zinc in the solution is 0.25-10.0% and the content of acid is 10-90%. The preparation may additionally contain an additive perfume, for example an ethyl ester of the corresponding alpha-chlorocarboxylic acid. The treatment method consists in that 2-5 doses of the preparation, which has been precooled to 10-15°С, are applied to the affected skin portion with a delay of 1-3 mins between the first and subsequent applications of the preparation. The preparations are stable on storage.
CN101273991B Applications of tetrahydroindolone/tetrahydroindazolone/tetrahydrocarbazole derivatives and salts thereof in preparation of antiviral medicine The invention relates to an application of tetrahydroindolone/ tetrahydroindazolone/ tetrahydrocarbazole derivatives and salts thereof in the preparation of antiviral drugs. The tetrahydroindolone derivatives, the tetrahydroindazolone derivatives or the tetrahydrocarbazole derivatives, as well as the salts thereof of the invention have anti-viral functions, and the virus comprises I-typed and II-typed herpes virus, coxsackie virus type 3 (CVB3) and hepatitis B virus.
US20050032779 enzyme inhibitors such as 2-[4-(4-Dimethylaminophenyl)piperazin-1-yl]4,5-dihydroimidazo[4,5,1-ij]quinolin-6-one, used for treating or preventing disorders in which poly/ADP-ribose/ polymerase is involved The invention relates to benzimidazole derivatives of general formula in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compounds of formula (I) comprising a secondary or tertiary amine; R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, optionally substituted C3-C7 heterocycloalkyl, —(CH2)p-heteroaryl, heteroaryl-carbonyl, phenylcarbonyl, (C1-C6)alkylcarbonyl, —(CH2)pCOOR, optionally substituted phenylsulphonyl or optionally substituted —(CH2)p-phenyl group, and, when X represents a carbon atom: R3 represents a hydrogen atom or a group —NR5R6, —N(R5)3 +, —NHCOR7, —CONHR5, —COR7, —NHCONH2, —OH or —CH2OH, R4 represents a hydrogen atom or an optionally substituted —(CH2)p-phenyl, —(CH2)p-heteroaryl or —(CH2)tNR7R8 group. Preparation process and therapeutic application.
CN101850028A Composition with function of relieving visual fatigue The invention discloses a composition with a function of relieving visual fatigue, which is prepared mainly with the following raw materials in parts by weight: 30-90 parts of European bilberry extract, 20-60 parts of ginkgo biloba extract, 25-75 parts of wolfberry extract, 17.5-52.5 parts of DHA powder, :0.055-0.165 part of vitamin A and 7.25-21.75 parts of vitamin C. Since the European bilberry extract, the ginkgo biloba extract, the wolfberry extract, the DHA powder, the vitamin A and the vitamin C are used as the main raw materials, the invention has the advantages of natural raw materials, balanced ratio, easy absorption, high pertinence and the like, and can improve the dry eyes and relieve the visual fatigue. Moreover, the invention is applicable to the majority of people due to the good healthcare function of relieving the visual fatigue.
US20050090558 Suppressing immune response in a mammal comprising accelerating lymphocyte homing (ALH) to any of mesenteric or peripheral lymph tissues or Peyer's patches by administering an ALH-immunosuppressive compound The methods and compositions of the invention and the compounds used in the invention involve a novel immunosuppression mechanism, accelerated lymphocyte homing immunosuppression (ALH-immunosuppression). For example, the compound FTY720 specifically directs lymphocytes to the peripheral lymph nodes, mesenteric lymph nodes, and Peyer's patches. By reversibly sequestering lymphocytes in these tissues, the compounds can inhibit an immune response in a mammal. Understanding these mechanisms provides a novel immunosuppression therapy that can synergistically interact with other immunosuppressive compounds. Screening methods for identifying similar ALH-immunosuppression compounds are also described. The invention allows better treatments and therapies wherever an immunosuppression regimen is desired.
CN102218061B Application of penehyclidine hydrochloride in preparation of medicine for treating motion sickness The invention discloses application of penehyclidine hydrochloride in preparation of a medicine for treating motion sickness; motion sickness is a joint name of train sickness, sea sickness, aviation sickness and other sickness caused by swinging, bumping, rotation, deceleration movement and the like due to various reasons. The medicine for treating motion sickness is tablets, granules, capsules or patches and other pharmaceutical preparations which are prepared by adopting the penehyclidine hydrochloride composition as a main component and adding pharmaceutically acceptable auxiliary components, wherein the weight ratio of the penehyclidine hydrochloride to the auxiliary components is 1: 1-1:400. According to the invention, the application field of the penehyclidine hydrochloride is widened, a novel medicine is provided for special group with motion sickness, the untoward effects and uncomfortableness brought to people by taking the conventional medicine for treating motion sickness are avoided; furthermore, the medicine is long in effective time, rapid in taking effect and smaller in dosage, and not only troubles caused by taking the medicine are reduced, but also the incidence of the untoward effects are also greatly reduced.
CN102614214A Composite povidone iodine tablet and preparation method thereof The invention belongs to the technical field of disinfectors and particularly relates to a composite povidone iodine tablet and a preparation method thereof. The composite povidone iodine tablet comprises the following components in parts by weight: 5 to 50 parts of povidone iodine, 5 to 30 parts of heat-releasing covering agent, 10 to 30 parts of effervescing agent, 15 to 40 parts of acidulant, 0 to 8 parts of synergistic agent and 5 to 25 parts of filler, wherein the heat-releasing covering agent is any one of or a mixture of anhydrous magnesium chloride and anhydrous calcium chloride; the effervescing agent is any one of or a mixture of sodium bicarbonate, sodium carbonate and magnesium bicarbonate; the acidulant is any one of or a mixture of citric acid, tartaric acid, sulfamic acid and sodium bisulfate; the synergistic agent is any one of or a mixture of sodium dodecyl sulfate, ethoxy modified polytrisiloxane powder and boric acid; and the filler is any one of or a mixture of sodium sulfate and sodium chloride. The composite povidone iodine tablet is stable, safe, corrosion-resistant, high in dissolution rate and reaction conversion rate and convenient to use.
CA2625906C Lazaroids-based compositions and methods for preventing adhesion formation using the same Compositions and method for the minimization or prevention of adhesion formation, whereby an effective amount of at least one lazaroid compound, preferably one of general formula (I), wherein R represents a formula (Ia) or (Ib), or formula (II), wherein R represents H or CH3; R1 represents formula (Ia) or formula (IIa), wherein R2, R3, R4, and R5 independently represent H or NR6R7, wherein R6 and R7 independently represent H and C1-C6 alkyl is administered for a period of time sufficient to permit tissue repair. The compound of general formulae (I) or (II) is preferably administered in conjunction with a delivery vehicle (e.g., microcapsules, microspheres, biodegradable polymer films, lipid-based delivery systems such as liposomes and lipid foams, viscous instillates and absorbable mechanical barriers) useful for maintaining local concentrations of the compound at an effective level.
CA2510985A1 Pharmaceutical formulations for the safe administration of drugs used in the treatment of drug addiction and processes for obtaining the same The present invention provides safe pharmaceutical formulations for drugs used in the treatment of drug addiction, namely formulations which render the abusive administration of the drug contained in these formulations not feasible, together with processes for obtaining said formulations.
DE102006008730A1 Use of cosmetic or dermatological preparation in the form of oil-in-emulsion comprising hydroxymatairesinol for the tightening and/or strengthening of the skin, preferably for cellulite Use of a cosmetic or dermatological preparation in the form of oil-in-emulsion comprising hydroxymatairesinol for the tightening and/or strengthening of the skin. - ACTIVITY : Dermatological. - MECHANISM OF ACTION : None given.
WO2009151770A3 Colchicine solid-state forms; methods of making; and methods of use thereof Disclosed are new colchicine solid-state forms, methods of preparing the solid-state forms, as well as formulations prepared therefrom and uses thereof.
WO2010148390A2 Polyamine transport inhibitors as novel therapeutics Novel polyamine transport inhibitors have been synthesized and demonstrated to block the uptake of native polyamines into human cancer cells. A combination therapy of the transport inhibitor and DFMO (a drug which blocks polyamine biosynthesis) provided synergistic activity against a metastatic human colon cancer cell line. The strategy uses polyamine depletion and polyamine metabolism to generate reactive oxygen species within cells as a novel way to treat cancers. This approach may be implemented for widespread use in the treatment of diseases which rely upon polyamine transport activity for proliferation.
US7432293 Heterocyclic compounds useful as Nurr-1 activators The present invention relates to compounds of formula (I): wherein R1 is hydroxy, C1-4 alkoxy, amino, C1-4 alkyl-amino, di C1-4alkylamino, benzyloxy or C2-C7 alkanoyl, R2 is C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxy C1-4alkoxy, CF3, halogen, C1-4alkylamino, di C1-4alkylamino, di C1-4 alkylamino C1-4 alkoxy or N—C1-4 alkoxy C1-4 alkyl-N—C1-4 alkylamino, N—C1-4 alkyl-piperazinyl, morpholinyl or pyrrolidinyl-C1-4 alkoxy, wherein the C1-4 alkyl radicals in R2 are optionally further substituted by C1-4 alkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3, X is O, Y is CH, Z is N and W is CH, (b) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3 or chloro, X is N, Y is O, Z is CH and W is CH, (c) R1 is not hydroxy when R2 is CF3, X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them.
WO2006068591A1 Novel pyrazole derivatives and their use as modulators of nicotinic acetylcholine receptors Compounds of Formula I: wherein A1, A2, D and E are as described in the specification, pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission.
CN1857469A Arasaponin composition preparation and its preparing process The present invention relates to compound preparation with arasaponin composition as main component for treating cardiac and cerebral vascular diseases. The arasaponin composition contains total haw arasaponin in 1-99 wt% and haw stem and leaf total phenolic acid, gingko leaf flavonid, sowthistle-leaf ixeris flavonid, total paeoniflorin or seabuckthorn flavonid in 1-99 wt%, and is compounded with pharmaceutically acceptable supplementary material to prepare pharmaceutically acceptable preparations. The medicine of the present invention is used in preventing and treating cardiac and cerebral vascular diseases, senile dementia, and other diseases.
WO2013135147A1 Use of substituted diphenylamine compounds in preparing anti-tumour drugs Provided is the use of substituted diphenylamine compounds of general formula I in preparing anti-tumour drugs. The compounds of general formula I have good anti-tumour activity, especially suitable for treating or relieving cancers caused by tumour cells in tissues and organs in a human body. The cancers preferably are colon cancer, lymphoma, lung cancer, esophagus cancer, breast cancer, central nervous system tumor, melanoma, ovarian cancer, cervical cancer, renal cancer, leukemia, prostate cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, pharyngeal cancer or gastric cancer etc. The structure of the compound of general formula I is shown in formula (I).
CA2630935A1 Beta glycolipids as immuno-modulators The present invention relates to a process for the modulation of the Th1/Th2 cell balance toward anti-inflammatory cytokine producing cells, in a subject suffering from an immune related disorder. The process of the invention comprises the step of increasing the intracellular, extra-cellular or serum level of a naturally occurring .beta.-glycolipid in a subject in need thereof. The invention further relates to methods for the treatment of a subject suffering from an immune-related disease. Therapeutic compositions and method for the preparation of these compositions are also provided
CN101103996A Electrolyte nutrition intensifier The invention provides an electrolyte nutrition enhancer which mainly contains kalium, calcium and magnesium and various vitamins. The electrolyte nutrition enhancer of the invention can effectively prevent a body builder from hypokalemia and jerk normally occurred before a competition, and can improve the fullness degree of muscles of the body builder to some extend. In addition, the electrolyte nutrition enhancer can be used to complement electrolyte and prevent functional disorders and lower resistance caused by lack of electrolyte for wide hypertensive slimmers.
CN1864682A In-vitro in-vivo drug release characteristics of various drug pills in compound anti-tuberculosis preparation and application thereof The present invention is that on the basis of rifampicin and isoniazide micro pill preparation of patent No. 03101211.6, the release status of the micro pill inside solution in specific conditions and the human body's pharmacokinetic characteristic of the micro pill in human body as the tested object are measured according to the method of Chinese pharmacopoeia.
WO2006062424A3 Use of 3-hydroxy-3-methylbutyrate alone or in combination with alpha-ketoglutarate in the growth and mineralisation of the osteo-skeletal system The invention dissolves the problem of the pharmaceutical preparation affecting the processes of the growth and the mineralisation of the osteo-skeletal system in the physiology and in the osteochondropathy in the matured people and animals. The essence of the invention is that 3-hydroxy-3-methylbutyrate (HMB) and its derivatives such keto-isokaproic acid (KIC) and leucin and isoleucine are used as chemical compound in a dose 0.001-1 g/kg/day, alone or in combination with alpha-ketoglutarate (AKG) or/and glutamines or/and glutamate or/and alpha- ketoglutarate of ornithine or/and dipeptides of glutamine and other amino acids or/and tripeptides of glutamine and other amino acids or/and di- and tripeptides of glutamate with other amino acid, or/and mono- and bivalent metal salts and other alpha-keto of glutarate or/and glutamine or/and glutamate or/and ornithine of alpha-ketoglutarate, in a dose 0.001-1 g/kg/day for producing of the curative preparation, functional and medical food.
CN101138547A Carthamus tinctorius yellow colour injection and method of preparing the same The present invention provides a stable injection preparation of the safflor yellow, which provides the water injection and the infusion. The injection preparation provided by the present invention has excellent stability, which resolves the stability problem requiring being resolved for a long period.
CN101323649B Method for extracting mushroom polysaccharide by using ultra-high pressure The invention discloses a method for extracting shiitake polysaccharides from shiitakes, which overcomes the defects that the existing extracting method requires long time, has low efficiency and high energy consumption and damages active ingredients of the shiitake polysaccharides. The proposal adopted by the invention comprises the following steps of: crushing the selected dry shiitakes, addingextract, processing under super-high pressure, filtering, concentrating in vacuum, precipitating with alcohol, drying and finally obtaining shiitake polysaccharides. The high pressure is adopted by the invention to hold or relieve pressure of the shiitake extract, increase the differences between osmotic pressures in and out of cells and change the structure of cells, thereby easily dissolving out effective ingredients, keeping the physiologically active ingredients unchanged, killing a part of microorganisms by high-pressure processing and finishing extraction and sterilization in one step. Being a cold extracting technique, the super-high-pressure extracting method generates no high temperature during the whole extraction process, shortens the extracting time to a few minutes, conservesthe effective ingredients, and has significant economic benefits and broad prospect of market development.
US20080188490 e.g. 1-(3-Chloro-phenylethynyl)-3-(3,4-difluoro-phenylamino)-cyclohexanol; metabotropic glutamate receptors modulator/antagonist; The invention provides compounds of formula (I) wherein the substituents are as defined in the specification, to processes for their preparation and corresponding intermediates, and their use as pharmaceuticals.
WO2007068577A1 Use of naveglitazar for preparing a pharmaceutical composition for use in the treatment of dermatological conditions The invention relates to the use of at least one compound chosen from 2-methoxy-3-[4-[3-(4-phenoxyphenoxy)propoxy]phenyl]propanoic acid, one of its isomers, in particular optical isomers, and/or its pharmaceutically acceptable salts, for preparing a pharmaceutical composition for use in treating dermatological conditions.
CN101152491A Alopecia treating medicine, preparing method and uses of the same The present invention relates to a medicine for curing alopecia and the preparation method and purpose; the raw materials for preparing the medicines are medicinal medlar, prepared rhizome of rehmannia, tube of multiflower knotweed, glossy privet fruit, cornel, yam, herb of yerbadetajo, Tuckahoe, oriental water plantain rhizome, moutan bark and sticky rice; the auxiliary materials are alcohol and honey; a small amount of vitamin A is added in the effective components; the raw materials are mixed and immersed in the alcohol; and then the mixture is mixed and compressed to extract the alcohol solution; the alcohol solution is put in a sealed container with consistent temperature and then the pressure is reduced and the alcohol solution is distilled to remove the alcohol which is used as the menstruum; the medicine obtained is made into pill, capsule or troche with conventional preparation method. The oral medicine can yield obvious curative effect in a short time; the medicine is innocuous and has no side effect; moreover, the price is low and the curative effect is obvious; in this way, the medicine is fit for consumers of various strata.
WO2012133693A1 Pharmaceutical combination for diabetes treatment [Problem] To provide a novel pharmaceutical combination that is useful for treating type II diabetes. [Solution] The present invention provides: a pharmaceutical useful for treating type-II diabetes, the pharmaceutical being composed of a combination of mitiglinide, which is an insulin secretion promoter, or a pharmacologically permitted salt thereof and a DPP-IV inhibitor; and a treatment method that uses the pharmaceutical. This pharmaceutical combination exhibits significant lowering of blood glucose without intensifying interactive side effects, and is extremely useful as an agent for reducing postprandial blood glucose excursion in type II diabetes.
US6906094 1,2,4-tribsubstituted benzenes as inhibitors of 15-lipoxygenase The present invention provides compounds of formula (I) wherein R, Z, Y, W, R5, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.
CN102659783A N-substituted sophora flavescens olefine acid derivative as well as preparation method and application thereof The invention relates to an N-substituted sophora flavescens olefine acid derivative represented by a general formula IA or IB, a preparation method thereof, a medicine composite containing the derivative, a method for utilizing the derivative to treat diseases caused by Coxsackie B viruses, and an application of the derivative to prepare a medicine for treating the diseases caused by the Coxsackie B viruses.
CN101972249A Application of methazolamide to preparation of medicament for treating plateau fatigue The invention relates to the application of methazolamide to the preparation of an anti-fatigue medicament taken under a plateau low-oxygen environment. The anti-fatigue medicament which is prepared from the methazolamide and taken under the plateau low-oxygen environment has the effects of enhancing exercise tolerance, delaying the occurrence of fatigue and accelerating fatigue elimination under the plateau environment and has the advantages of convenient source, small taking dose and small toxic or side effect.
WO2007103554A1 Quinoline and isoquinoline derivatives as phosphodiesterase 10 inhibitors The present invention is directed to certain quinoline and isoquinoline compounds that are PDElO inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDElO enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
WO2011096374A1 Novel iodobenzyl-bleomycin compound Provided is a novel iodobenzyl-bleomycin compound. Also provided are metal complexes that consist of the iodobenzyl-bleomycin compound and various metal atoms, such as an iodobenzyl-Co-bleomycin compound, that can accumulate on malignant tumors, and that have improved biological characteristics in terms of accumulability on malignant tumors compared to conventional compounds. Also provided are methods for synthesizing the iodobenzyl-bleomycin compound and the metal complexes of the iodobenzyl-bleomycin compound and various metal atoms. The novel iodobenzyl-bleomycin compound is synthesized by adding, to a terminal amino group of bleomycin, iodobenzyl iodide synthesized by using iodobenzyl alcohol and iodine as starting materials.
US20070123529 Substituted biphenyl compounds The invention relates to compound of formula (I) wherein: B represents hydrogen, COOR, CONRR′, or (C1-C6)alkyl substituted by COOR, CONRR′, or OR, G1 represents —X′—(CH2)n—X—(CH2)m—X″— chain wherein X, X′, X″, n and m are as defined in the description, Cy represents a grouping of formula (II) or (III): G2 represents alkylene chain as defined in the description, and A represents NRCOR′, NRCSR′, CONRR′, CSNRR′, NRCONR′R″, or NRCSNR′R″. and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.
CN102617517A Novel 7,10-O,O-dimethyl docetaxel derivatives and use thereof The invention relates to novel 7,10-O,O-dimethyl docetaxel derivatives and a use thereof. The novel 7,10-O,O-dimethyl docetaxel derivatives have a general structural formula shown in the patent specification. The novel 7,10-O,O-dimethyl docetaxel derivatives can be prepared into intravenous water-soluble preparations so that side effects of Tween-80 in an injection used clinically are eliminated and thus drug safety is improved. Results of an in-vitro cell experiment and an in-vivo animal experiment of novel 7,10-O,O-dimethyl docetaxel derivatives prove that the novel 7,10-O,O-dimethyl docetaxel derivatives have good effects on breast cancer, lung cancer or ovarian cancer. A preparation method of the novel 7,10-O,O-dimethyl docetaxel derivatives is simple and safe. The quality of the novel 7,10-O,O-dimethyl docetaxel derivatives can be controlled easily.
CN101371844A Sticking tablet for curing mouth ulcer using mometasone furoate as active component The invention relates to an oral sticking tablet used for treating human or animal dental ulcer; the oral sticking tablet consists of an adhesive layer containing active components and a water insoluble protective layer; the inactive component containing in the adhesive layer consists of a filling agent, an adhesive sustained-released agent and a lubricant that are applicable to tablet, and the water insoluble protective layer consists of polyacrylic acid resin and/or ethyl cellulose which can be used as protective coatings and a plasticizer, and the active component is momestasone furoate.
CN1800238A Aliphatic polyester-polyamino acids copolymer with biological function and its synthesis method The invention relates to a fatty group polyester-polyamino acid copolymer with biology function and its synthesis method in the field of macromole biological medicine material technique. The block copolymer comprises: the two block copolymer (A) of fatty group polyester -polyamino acid with biology function and three block copolymer (B), and polyoxyethylene-fatty group polyester-polyamino acid three block copolymer (C). The synthesis method comprises: synthesizing the block copolymer of the carboxylic which is protected by benzyl, doing catalytic reduction to the palladium wood coal or hydrolyzing hydrogen bromide to generate the corresponding polymer with free carboxyl, then using NHS (N- hydroxyl succinimide-sauba) to active the flank carboxyl of the polyamino acid section, reacting it with short peptide, sugar or drug with RGD to obtain the fatty group polyester-polyamino acid copolymer with biology function.
WO2014125121A1 Compounds and compositions for treating neurodegenerative diseases The present application relates to a composition comprising a selective androgen modulating compound of formula (I) and selective estrogen receptor β agonist of formula (II). The present application also relates to the use of a selective androgen modulating compound of formula (I) in combination with a selective estrogen receptor β agonist of formula (II) in the treatment or prevention of neurodegenerative diseases or disorders,such as Alzheimer's disease, Huntigton's disease, Parkinson's disease, depression, anxiety, multiple sclerosis, symptoms associated with or caused by multiple sclerosis, and acute or chronic pain.
CN102068695B Method for producing quadruple inactivated vaccine for newcastle disease, infectious bronchitis, avian influenza (H9 subtype) and infectious bursal disease The invention relates to a method for producing a quadruple inactivated vaccine for newcastle disease, infectious bronchitis, avian influenza (H9 subtype) and infectious bursal disease. In the method, the inactivated vaccine is prepared by adopting a newcastle disease virus La Sota strain, an infectious bronchitis virus M41 strain, an avian influenza virus (H9 subtype) YBF003 strain, and an Escherichia coli genetic engineering bacteria E. coil BL21/pET28a-VP2 strain which expresses an infectious bursal disease virus VP2 protein serving as production bacteria toxic species, a super concentration process and a high-quality adjuvant. After immunizing animals, antibodies are produced rapidly; the potency is high; the protection period is long; and the outbreak and the spreading of epidemic diseases are reduced.
US7247615 Nucleic acid encoding peptides which antagonist epitope against prostate specific antigen; anticancer agents This invention relates to isolated peptides comprising agonist epitopes of prostate-specific antigen (PSA). In various aspects, the invention relates to peptides comprising agonist epitopes of the PSA-3 cytotoxic T lymphocyte epitope, and nucleic acids encoding peptides that comprise PSA-3 agonist epitopes. Also related are probes, primers, and vectors comprising these nucleic acids, as well as host cells comprising these vectors, and antibodies that bind to the PSA-3 agonist peptides. This invention further relates to diagnostic reagents and methods utilizing the disclosed nucleic acids or antibodies. The invention also relates to pharmaceutical compositions comprising the nucleic acids, host cells, and peptides of the invention, as well as methods of treatment or prevention of prostate cancer employing such compositions, for example, for peptide-mediated, cell-mediated, and vector-mediated immunotherapies.
US20090023786 Histone Deacetylase Inhibitor Prodrugs The present invention is directed to prodrugs of hydroxamic acid based histone deacetylase (HDAC) inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The prodrugs are acylated derivatives having increased aqueous solubility and cellular permeability as compared with the free hydroxamic acid, and are useful for inhibiting HDACs, and for selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the prodrugs of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The prodrugs of the invention are also useful in the prevention and treatment of thioredoxin (TRX)-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
CN102000045A Application of resveratrol in preparing medicament for preventing and treating radiation induced depigmentation skin disease The invention discloses application of resveratrol in preparing a medicament for preventing and treating radiation induced depigmentation skin disease. A path for treating occurrence and development of ionizing radiation induced leucoderma is established by treating a radiation induced IRM-2 mouse leucoderma model with resveratrol. Mice irradiated by 6Gy after 30 days orally take the medicament for 15 days, and then the result shows that the depigmentation inhibiting rate of the medicament administration group reaches 40% compared with the control group, so the medicament has remarkable effect. Pathological detection results show that hair follicles of the pathological change part of the mice of the resveratrol administration group are distributed more densely, and the distribution of melanin is obviously wider than that of an irradiation group and a normal group. The immune indexes of the mice of the resveratrol administration group, such as peripheral blood leukocyte number, femoral nucleated cell number, CFU-S (colony forming unit-spleen), CFU-GM (colony forming unit-granulocyte and monocyte) and the like, are slightly higher than those of the irradiation group, so the resveratrol has certain protection effect on hematopoiesis and immunologic function of the irradiated mice. The results show that the resveratrol has positive prevention and treatment effect on the occurrence and development of the radiation induced mice leucoderma.
US20080026072 glycoproteins having alpha 1,4-linked N-acetylglucosamine residue from milk of mammal containing carrier polypeptide with alpha 1,4-N-acetylglucosaminyl transferase; for treatment or prevention of gastric ulcers Compositions useful for inhibiting the growth of bacteria, including bacteria that can cause gastric ulcers, are provided. In addition, transgenic organism that can produce such compositions are provided. Methods of using the compositions to treat or prevent gastric ulcers in a subject, including a human subject, also are provided.
US20090198145 Compositions, methods, and systems for rapid induction and maintenance of continuous rem sleep Compositions, kits, methods, and systems to induce, maintain, monitor, and interpret a continuous, un-fragmented REM sleep state in humans, generate dreams, recover sleep, create brain neuronal plasticity and activate the brain for cognition enhancement and mood stabilization are described. If potentially combined with other medications, a platform is provided to develop new research and therapies in many fields treating the human brain. The procedure reliably and quickly generates a Continuous REM Sleep cycle of pre-determined time or indefinite duration depending on therapeutic goals, allowing the patient to experience a qualitatively superior dream sleep in a shortened period of time compared to a natural sleep cycle. Profuse positive (pleasant) dreams are produced as well. REM sleep, dreams and sleep recovery can be reliably generated, and various sleep, psychological and neurological illnesses and disorders can be treated or prevented either solely by this method or in combination with additional agents.
US20100317698 Polysubstituted Pyridinylaminoalkylene- and Pyridinyloxyalkylene-Cyclopropanamine Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them Compounds of formula (I): wherein: n represents an integer of from 1 to 6 inclusive, X represents an oxygen atom or an NR6 group, Y represents a carbon atom or a nitrogen atom, Z represents a carbon atom or a nitrogen atom, R1 and R2 represent a hydrogen atom or an alkyl or arylalkyl group, R3 and R4 represent a hydrogen atom or an alkyl group, R5 represents a hydrogen atom or an alkyl, halogen, hydroxy, alkoxy, cyano, nitro, acyl, alkoxycarbonyl, trihaloalkyl, trihaloalkoxy or optionally substituted amino group, R6 represents a hydrogen atom or an alkyl or arylalkyl group, Ra, Rb, Rc, Rd and Re are as defined in the description. Medicinal products containing the same which are useful as specific nicotinic ligands of α4β2 receptors.
CN1623538A Tanshinone II A sulfonic acid or tanshinone II A sodium sulfonate freeze-dried powder injection and its preparation method A freeze-dried powder injection of tanshinone IIA-sulfonic acid (or sodium sulfonate) for treating coronary heart disease, angina pectoris, myocardial infarction, atherosclerosis, thrombus, etc is prepared from the tanshinone IIA-sulfonic acid (or sodium sulfonate) and at least one pharmacologically acceptable carrier chosen from excipient, pH regulator, antioxidizing agent and stabilizer. Its advantages are high curative effect and high stability.
US20080138350 Process for use of fluoroquinolones to reduce or modulate inflammation due to eye disease or ophthalmic surgery The present invention provides a safer and more effective way to treat ophthalmic disease and to perform ophthalmic surgeries while reducing the risk of vision loss due to the inflammatory response in the eye. The invention generally relates to the use of fluoroquinolones to reduce inflammation due to ophthalmic disease or ophthalmic surgery, including treatments for macular degeneration, diabetes, and vascular ischemic diseases, and other ophthalmic diseases. One aspect of the present invention involves using an anti-VEGF medication along with moxifloxacin in treating ophthalmic disease and in reducing inflammatory response in the eye following surgery for treating diseases like wet macular degeneration. Another aspect of the present invention involves delivering a fluoroquinolone combination to the eye in a sustained delivery application or device.
WO2013170655A1 High penetration prodrug compositions and pharmaceutical composition thereof for treatment of pulmonary conditions The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) for treatment of pulmonary conditions (e.g. asthma). The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
WO2008067120A3 (s)-phenyl(heterocycle)methanol-based compounds, compositions comprising them and methods of their use Multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use are described. Compounds described include those of formula (I).
CN101190233A Erythromycin chewable tablets for dog or cat The invention discloses an erythromycin chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the existing tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 10 to 30 percent of erythromycin.
US20080318880 Neoadjuvant treatment of Breast Cancer Neoadjuvant treatment of inflammatory or T3 to T4 breast cancer is carried out by administering to such patients a number of cycles of chemotherapy treatment in which DPPE first is administered followed by a combination of anthracyclines and taxanes.
EP2595957A1 Pyridin- 2 - yl sulfanyl acid esters and process for the preparation thereof The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HUVEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS-Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure la, R1 = H, R2 = H, R3 = CH2COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.
US20120039963 3-(2-Dimethlaminomethyl Cyclohexyl)Phenol Retard Formulation A pharmaceutical dosage form for controlled release of the active substance 3-(2-dimethylaminomethylcyclohexyl)-phenol, preferably (1R,2R)-3-(2-dimethylaminomethylcyclohexyl)-phenol, or a pharmaceutically acceptable salt thereof, which dosage form (i) in vivo produces a peak plasma level of the active substance after 2 to 10 hours, and/or (ii) in vitro releases 3.0 to 37 percent by weight of the active substance originally contained in the dosage form after one-half hour, 5.0 to 56 percent by weight after one hour, 10 to 77 percent by weight after two hours, 15 to 88 percent by weight after 3 hours, at least 30 percent by weight after six hours, at least 50 percent by weight after 12 hours, at least 70 percent by weight after 18 hours, and at least 80 percent by weight after 24 hours when measured according to the European pharmacopoeia using a blade mixer in preferably 900 ml of a buffer solution at a pH value of 6.9, a temperature of 37° C., and 75 rpm.
US7332276 Administering steroid compound The SOST gene gives rise to sclerostin, a protein that leads to apoptosis of bone progenitor cells. The invention provides antagonists to the sclerostin protein, and methods for identifying new sclerostin antagonists. The invention also provides molecules that can depress expression of the SOST gene, as well as methods for identifying such molecules. Such molecules and antagonists are useful for increasing bone mineralization in mammals, for example, in the treatment of osteoporosis.
CN101235097A Method for extracting polysaccharide from angelica and application thereof The invention discloses a method for extracting polysaccharide from chiretta and an application, which comprises breaking dry chiretta via a breaker into powder, arranging into an extraction pot, adding ligarine to reflux and defat, adding distilled water into defatted residues to extract, processing alcohol precipitation and centrifugation to obtain deposits, removing protein, processing acid hydrolysis and gel chromatography separation, freezing and drying to obtain active chiretta polysaccharide. The invention further discloses an application of the active chiretta polysaccharide in the ostarthritis prevention or treatment drug preparation. The invention has definite effective components, definite curative effect, non toxic side effect and easy process.
EP2724723A1 Tegaserod for use in the treatment of nerve injuries This invention relates to novel pharmaceutical composition comprising tegaserod and/or a pharmaceutically acceptable salt thereof for the treatment of neurological injuries, such as traumatic and chronic lesions of the central and peripheral nervous systems and for regenerating damaged nerves and nerve function. The pharmaceutical compositions of the invention can also be used for treatment and/or prevention of acute and chronic injuries to the central and peripheral nervous systems, for promoting growth and/or regrowth of nerves and enhancing formation of synapses and synaptic plasticity, and for neuroprotection.
US6930101 Thiazolopyrimidines useful as TNFα inhibitors The invention provides derivatives of thiazolo[4,5-dl]pyrimidine and their use as inhibitors of proinflammatory cytokines.
US7169817 Treatment and/or prevention of diseases or disorders mediated by lymphocyte interactions. The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them. Compounds according to the present invention are based upon the chemical formula: wherein the substituents have the values mentioned herein.
CA2263921C Oral delayed immediate release formulation and method of preparation therefor The invention relates to an Oral Delayed Immediate Release formulation comprising a compressed core containing one or more active substances surrounded with a coating, wherein release of active substance from the core is caused by rupture of the coating after a definite lag-time, said core comprising one or more immediate release carriers and having no substantial swelling properties upon exposure to gastrointestinal fluids. The invention further relates to formulations containing an Immediate Release formulation combined with one or more Oral Delayed Immediate Release formulations with different lag-times and to a method of preparing an Oral Delayed Immediate Release formulation. The Oral Delayed Immediate Release formulation may be used for the application of active substances whenever a certain lag-time before release is advantageous, such as in the case of anti-asthmatics, anti-emetics, cardiotonics, vasodilators, anti-vertigo and anti-ménière compounds, anti-hypertensives, sedatives, anti-depressants, anti-anxiety compounds, cortico-steroids, general anti-inflammatory compounds, anti-inflammatory compounds for gastrointestinal use, anti-ulceratives, analgetics, anti-aritmics, anti-rheumatics, anti-arthritic compounds and anti-angina compounds. The Oral Delayed Immediate Release formulation may also be used for the application of biological active compounds such as proteins, peptides, enzymes, vaccines and oligonucleotides.
WO2013121034A1 Methods and pharmaceutical compositions for reducing adipose tissue inflammation The present invention relates to an inhibitor of interferon regulatory factor 5 (IRF5) activity or expression for use in a method for reducing adipose tissue inflammation in a subject. The present invention also relates to a method for screening a plurality of candidate compounds useful for reducing adipose tissue inflammation comprising the steps consisting of (a) testing each of the candidate compounds for its ability to inhibit interferon regulatory factor 5 activity or expression and (b) and positively selecting the candidate compounds capable of inhibiting said interferon regulatory factor 5 activity or expression.
CN101602778A CA-4P, preparation method and pharmaceutical composition thereof The invention provides a CA-4P suiting for a pharmaceutic purpose and having a special quality limit and also relates to a preparation method and the pharmaceutic purpose thereof as well as a pharmaceutical composition containing the same.
CN103751253A Veterinary pharmaceutical composition for treating swine fever as well as preparation method and application thereof The invention provides a veterinary pharmaceutical composition for treating the swine fever. The veterinary pharmaceutical composition is a preparation prepared from the following crude drugs in parts by weight: 1-3 parts of an astragalus polysaccharide extract and 4-6 parts of a honeysuckle extract. The invention further provides a preparation method and application of the veterinary pharmaceutical composition. Through combined utilization of the astragalus polysaccharide extract and the honeysuckle extract prepared with specific methods, the veterinary pharmaceutical composition plays the role of synergistic interaction, obviously improves the prevention of a single drug to the swine fever or curative activity, and provides a new choice for clinical medication.
CN101910152A 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors The present invention provides substituted bicyclic heteroaryl compounds, including, for example, 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines that modulate the activity of kinases and are useful in the treatment of diseases related to activity of kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
US20080227750 Complex of glycan and galactin accumulated on cell surfaces; therapy, prevention of autoimmune diseases The invention relates to isolated complexes comprising one or more galectin associated with a Mgat5 modified glycan or polylactosamine modified glycan, and isolated lectin-Mgt5 modified glycan lattice comprising an array of mulitvalent interactions among lectins, Mgat5 modified glycans, polylactosamine modified glycans, and/or glycoproteins. Methods for evaluating a test compound for its ability to regulate receptor clustering through glycans on cell surfaces; and methods for regulating receptor clustering on cell surfaces comprising altering glycans on the cell surface associated with receptor clustering are also disclosed.
EP0948646B1 Methods for identifying genes essential to the growth of an organism The present invention provides methods for identifying genes essential to the growth of an organism using a grid prepared from a genomic library of a selected organism. Genes identified as essential by this method and proteins encoded thereby are also provided. In addition, methods of using these genes and proteins encoded thereby are disclosed.
US20080206316 Nutraceutical; chromium atoms bonded to fatty acids; linoleic acid, linolenic acid, gamma-linolenic acid, arachidonic acid; and transition metal, an alkaline metal, alkaline earth metal, rare earth metal, or metalloid; nutritional supplements, food stuffs, and pharmaceutical compositions Disclosed are compounds comprising one or more chromium atoms bonded to one or more fatty acids. Also disclosed are nutritional supplements, pharmaceutical formulations, delivery devices, and foodstuffs comprising the disclosed compounds. Methods of using the disclosed compounds and compositions to improve health are also disclosed.
WO2012025857A1 Cycloalkyl methoxybenzyl phenyl pyran derivatives as sodium dependent glucose co transporter (sglt2) inhibitors The invention relates to the cycloalkyl methoxybenzyl phenyl pyran derivatives as Sodium dependent glucose co transporter (SGLT) inhibitors, particularly SGLT2 and method of treating diseases, conditions and/or disorders inhibited by SGLT2 with them, and processes for preparing them.
WO2007014524A1 Erianin salts, their preparation methods and pharmaceutical compositions containing the same The invention discloses erianin salts of formula (I) and their preparation methods, wherein R is a salt formed by the monovalence acid radical of inorganic oxy acid or organic acid with metal, ammonium salt or organic amine. The invention also discloses pharmaceutical compositions containing erianin salts. Compared with erianin, the solubility of said erianin salts is significantly increased, thereby enhancing bioavailability and exhibiting better antitumor acitivity.
CN103054793A Propranolol hydrochloride cream used for treating infantile hemangioma, and preparation method thereof The invention discloses a propranolol hydrochloride cream used for treating infantile hemangioma, and a preparation method thereof. The cream comprises the components of, by weight, 0.8-1.2% of propranolol hydrochloride, 5.5-8% of octadecanol, 5.5-8% of glycerol monostearate, 5.5-8% of stearic acid, 7.5-10.5% of liquid paraffin, 7.5-10.5% of glycerol, 7.5-10.5% of propylene glycol, 1.5-2.5% of an emulsifier, 0.4-0.6% of a penetration enhancer, 0.08-0.12% of a preservative, and balance of water. The propranolol hydrochloride cream provided by the invention has good stability, and an effective duration of at least 24 months. The cream can directly act upon an infection site, such that local medicine concentration is high, and adverse reactions caused by oral administration or intravenous administration can be avoided. With the cream, medicine effect can be maximized, and medicine side effect can be reduced. The cream has a definite effect, and is suitable for industrialized large-scale productions. The cream is used for treating hemangioma and is especially suitable for treating infantile hemangioma.
US20140079662 Compositions and methods for treating respiratory disorders with doxofilline COMPOSITONS AND METHODS FOR TREATING RESPIRATORY DISORDERS WITH DOXOFILLINE.
CN102008699A Medicine for treating barrenness The invention discloses a medicine for treating barreness. The medicine comprises formulas A and B, wherein the formula A is composed of the followings bulk pharmaceutical chemicals: rhizoma atractylodis, angelica, safflower, fructus evodiae, motherwort, rhizoma cyperi, Szechuan lovage rhizome, the seed of cowherb, rhizome pinelliae preparata, baked ginger, peach kernel, beautiful sweetgum Fruit, dried orange peel and radix bupleuri; and the formula B is composed of the following bulk pharmaceutical chemicals: Salvia miltiorrhiza, dogwood, cornu cervi degelatinatum, safflower, epimedium sagittatum, root of common peony, radix paeoniae alba, radix dipsaci, rehmanniae vaporata, angelica, amethyst, Chinese yam, the seed of Chinese dodder, pinene and rhizoma curculiginis. In the formulas provided by the invention, modulation is carried out firstly, and stagnation of qi activity and phlegm stasis block are treated by regulating the flow of vital energy and removing obstruction, and the medicine can tonify kidney and support Yang after menstrual period, thus the medicine can treat the barreness.
WO2006128058A3 Thyromimetics for the treatment of fatty liver diseases The present invention is directed toward the use of thyromimetic compounds that are thyroid receptor ligands, pharmaceutically acceptable salts thereof, and to prodrugs of these compounds for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis.
WO2013184878A1 Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
CN1981871A Elemene externally-applied preparation and its use An exterior-applied elemene medicine with slow release and low irritation is proportionally prepared from elemene, organic solvent, medicinal matrix, and the additive chosen from hyaluronic acid, sodium hyaluronate gel, hyaluronidase, carbomer, and chitin. Its preparing process is also disclosed.
CN102210703B Dextran of polypeptide donkey-hide gelatin The invention provides dextran which is prepared from polypeptide donkey-hide gelatin composition with different weight-average molecular weights and compatible tryptophan, containing gelatin molecules with different molecular weights. The dextran is characterized in that: smaller molecules can be easily filtered from glomerulus so as to promote urine in early input stage; bigger molecules stay in blood vessels to prolong the expansion effect; and increase of the tryptophan can irritate synthesis of albumin of the tryptophan so as to supply massive lost plasma protein.
CN102600142A New application of peiminine in manufacturing gastric cancer multidrug resistance reversing medicaments The invention relates to new application of peiminine in manufacturing gastric cancer multidrug resistance reversing medicaments. The molecular formula and the molecular weight of peiminie are respectively C27H43NO3 and 429.63522. The beneficial effects provided by the invention are as follows: peiminine is used as a reserving agent; and cytotoxicity tests show that peiminine can obviously increase the sensitivity of drug resistance cells SGC7901/VCR on chemotherapeutics when being used together with commonly applied chemotherapeutics such as VCR (vincristine), ADR (adriamycin), CDDP (cis-platinum) and 5-Fu (5-fluorouracil). The result points out that when peiminie is applied with the chemotherapeutics to inhibit proliferation of the drug resistance cells, the proliferation capacity and the drug resistance level of the drug resistance cells are reduced, IC50 (half inhibitory concentration ) of the chemotherapeutics is reduced, and the cytotoxicity is increased. Therefore, peiminine can not only inhibit the proliferation of gastric cancer cells but also has the function of reserving gastric cancer multidrug resistance.
US20080096957 Albumin-Binding Conjugates Comprising a Fatty Acid and Peg The present invention provides an albumin-binding compound essentially of the following elements: a spacer group, a water-soluble bridging group, a fatty acid chain and an acidic group characterised in that the acidic group is attached to the distal end of the fatty acid chain. The invention also provides an albumin-binding compound to which one or more biologically active moieties are attached.
US20080090759 Methods and kits for predicting risk for preterm labor The invention is directed to kits and methods that allow one to predict the risk for preterm labor in a pregnant woman. The inventors have discovered that various extracellular matrix components can be detected in cervical secretions. The quantification of certain extracellular matrix proteins found within cervical secretions can be used as a diagnostic for the biomechanical state of the cervix, which indicates whether preterm labor is likely. Some extracellular matrix components that can be found in cervical secretions include decorin, thrombospondins and matrix metalloproteinases.
CN103479651A Application of Phyllanthoid A to in preparation of platelet increasing medicament The invention discloses an application of Phyllanthoid A to in preparation of a platelet increasing medicament, and belongs to the technical field of novel applications of medicaments. The Phyllanthoid A has good development and application prospects. The application of the Phyllanthoid A to in the preparation of the platelet increasing medicament in the invention belongs to a is disclosed for the first disclosuretime; moreover, the Phyllanthoid A has high platelet increasing activity and is a remarkable progress.
CN103520361A Compound lycopene preparation with immunity enhancement and chronic disease healthcare effects The invention relates to a compound lycopene preparation with immunity enhancement and chronic disease healthcare effects. A composition taking lycopene oil resin, selenium-enriched yeast and arginine as active ingredients is prepared into soft capsules in combination with pharmaceutically acceptable accessories, wherein the lycopene oil resin contains lycopene and safflower oil. According to the composition, the three raw materials, including lycopene oil resin, selenium-enriched yeast and arginine, are optimally and scientifically proportioned to achieve synergistic effects on the basis of the modern immunology theory and the free radical theory, so that the disease resisting function of an organism body can be excited, functions of a human immune system and a digestive system can be enhanced, and chronic diseases and sub-health diseases can be prevented and treated.
EP2587919A1 Methods for treating post traumatic stress disorder Compounds and compositions are described herein for treating post tramatic stress disorder.
EP1264821B1 Novel crystal of stilbene derivative and process for producing the same A IV-form crystal of (Z)-N-[2-methoxy-5-[2-(3,4,5-trimethoxyphenyl)vinyl]phenyl]-L-serine amide hydrochloride which can be obtained through a crystallization step employing a solvent containing at most 2 wt.% water and which, when examined by X-ray powder diffractometry, gives a pattern having peaks at least at 13.4°, 18.7°, 19.4°, and 22.5° (2υ). This compound is useful as an active ingredient for a carcinostatic agent. By the process, a crystal is obtained which has excellent properties desirable from the standpoint of the production of medicinal products, i.e., considerably reduced moisture adsorption and extremely high stability to water. Also provided are a process for producing the IV-form crystal and a method of using the crystal.
CN203075250U System for producing amino acid injection The utility model discloses a system for producing an amino acid injection. The system comprises five systems including a cleaning system, a configuring system, a filling system, a sealing system, a sterilizing system and a light inspection filling system, wherein weighting and preparing of raw and auxiliary materials are carried out strictly, and the requirement of controlling the temperature is high. An acid regulating system is used for limiting a PH value to be within 6.0-6.5, and adsorption bleaching is needed; and in a filling and sealing process, a novel process filling method of filling nitrogen is firstly adopted. After the technical scheme is adopted, the system has the advantages of stable content, good clarity, colorlessness, stability in color and the like.
US7276518 For therapy of neuropathic or chronic pain Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds.
CN102764260A Pharmaceutical composition of camptothecin derivative and preparation method thereof The invention relates to a pharmaceutical composition, which comprises (+)-(4S)-11-succinyl oxyethyl-4-ethyl-4-hydroxy-1H pyran[3',4',6,7]indolizine[1,2-b]quinoline-3,14-(4H,12H)-dione or its pharmaceutically acceptable salt, a stabilizing agent and a pH conditioning agent, wherein the pH value is 6.0-7.2.
US7598245 Pyruvate dehydrogenase kinase, c-KIT, cyclin-dependent kinases, Janus kinases, FLT3 kinase, AUR-2 kinase, tyrosine kinase; 1-(2-amino-4-pyridyl)-3-phenylaminotriazoles; combination therapy with antiallergens, immunomodulators, antiproliferative agents; Alzheimer's, Parkinson's, Multiple Sclerosis, asthma The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.
US20110064776 Dental composition containing organic nanotube Disclosed is a dental composition, comprising unsaturated double bond-containing monomers and/or oligomers, a catalytic amount of polymerization initiator to initiate polymerization, and a filler, wherein the dental composition comprises an organic nanotube containing an antibacterial or anticariogenic material to inhibit or prevent tooth decay. The dental composition comprises an organic nanotube containing an antibacterial or anticariogenic material, thus uniformly and continuously exhibiting anticariogenic and antibacterial activities, while avoiding deterioration in physical properties required for the dental material.
WO2012022120A1 Dihydropyrazole compounds Provided are a dihydropyrazole compound as represented by general formula (Ia), a pharmaceutically acceptable salt or isomer thereof, a preparation process thereof, a pharmaceutical preparation containing such compounds and the use thereof. The definitions of the various substituents in formula (Ia) are as described in the specification. The compounds can be used for treating and/or preventing renal injury, cardiovascular diseases, especially hypertension, and/or endocrine diseases.
DE102004002885A1 New pyrrole alkaloid daminin and its derivatives, are intracellular calcium ion concentration reducing neuroprotective agents useful for treating neurodegenerative diseases, e.g. Alzheimer's disease New pyrrole alkaloids (I) consist of the parent compound 1-(2-(pyrrol-3-ylcarbonyloxy)-ethyl)-pyridinium-3-carboxylate (designated daminin) and its derivatives. - Pyrrole alkaloids of formula (I) are new. - R1 - R11, X = H, optionally substituted 1-18C alkyl (including cycloalkyl), alkenyl, optionally substituted aryl (including heteroaryl), optionally substituted benzyl, acyl (e.g. CHO, COMe, COCCl3, fumaryl, maleyl, succinyl, COPh or branched, heteroatom-containing or aryl-substituted acyl), OH, SH, alkoxy (including cycloalkoxy, e.g. 1-4C alkoxy), alkylthio (e.g. SMe or SEt), substituted sulfonyl (e.g. SO3H, SO2Me, SO2CF3, SO2C6H4Me or SO2C6H4CH2Br), nitrogen substituent (e.g. NH2, NHR, NRR', NC or NO2), halo, CN or hetero-substituent; - R, R' = alkyl or aryl; - provided that (i) if R6 is different from R7, R4 is different from R5 or R1 - R3 or R8 - R11 are sterically hindered aryl groups, then (I) may be centro- or axially chiral, and all stereoisomers and racemic mixtures are included, (ii) two or more substituent groups may be linked to form aromatic, heteroaromatic or saturated rings and (iii) agelongin of formula (I; X = O-; R2 = Br; R1, R3 - R11 = H) is excluded. Independent claims are included for the preparation of (I). - ACTIVITY - Neuroprotective; cerebroprotective; nootropic; neuroleptic; antiparkinsonian. - MECHANISM OF ACTION - Reduction of intracellular calcium ion concentration. Daminin (Ia) reduced the increase in intracellular calcium ion concentration in cultured neurones caused by the N-methyl-D-asparate (NMDA) agonist L-glutamate. Pre-incubation of neurones with (Ia) at a concentation of 0.5, 1.0 or 3.0 mu g/ml for 5 minutes before incubation with L-glutamate caused dose-dependent inhibition of the L-glutamate-induced increase in the intracellular calcium ion concentration, the degree of inhibition being almost 100% using (Ia) at 3.0 mu g/ml.
WO2011113301A1 Self-emulsifying formulation of taxanes and preparation method thereof A self-emulsifying pharmaceutical composition for delivering taxanes is disclosed. It comprises taxane, oil, surfactant and ethanol, preferably also comprises lactic acid. The surfactant is phospholipid or polyoxyethylenated castor oil. When added into the glucose injection, the self-emulsifying pharmaceutical composition immediately forms a microemulsion with a particle size of 50-300 nm. The microemulsion is stable for more than 12 hours at room temperature.
WO2011156451A3 Compositions and methods for modulating toll-like receptor 2 activation A method of modulating angiogenesis, wound healing, hair growth, and/or an immune or inflammatory response in a tissue of a subject can include administering to tissue of the subject a therapeutically effective amount of an agent that promotes or inhibits TLR2 activation.
US20080261874 Point mutations; single or double alternation of tyrosine and aspartate residues; carcinoma; AIDS; gene therapy The invention provides the mutants and coding genes of trichosanthin (TCS). The mutants thereof are the TCS mutants with the single or double alternation of tyrosine-55 and aspartate-78 (counted from N-terminus), wherein the tyrosine-55 is mutated to an aliphatic amino acid and aspartate-78 is mutated to an amino acid with low hydrophilicity. This invention also relates to the application of TCS mutants and their coding genes in the drug development to treat carcinoma, AIDS and other diseases.
WO2011100267A1 Liquid composition comprising a non-menthol cooling agent and a thickener for treating a respiratory symptom The present disclosure describes methods for enhancing an overall cooling sensation of an oral mucosa comprising administering a liquid composition comprising a thickening agent and/or a mucoadhesive polymer, a non-menthol coolant; and contacting the oral mucosa with the liquid composition. The disclosure also describes the liquid compositions.
CN101732252B Tropisetron hydrochloride suspension injection The invention discloses a Tropisetron hydrochloride suspension injection, which is characterized by comprising the following components in parts by weight: 1 part of Tropisetron hydrochloride, 2.5-15 parts of surfactant, 0.1-5 parts of antioxidant and 5-40 parts of additive, wherein the surfactant is composed of sodium deoxycholate and polyvidone. Compared with the prior art, the Tropisetron hydrochloride suspension injection provided by the invention has unexpected effects, is mainly characterized by good quick solubility, clarity and stability, high bioavailability, little toxic or side effect and the like, and can be used for subcutaneous injection, intramuscular injection and intravenous injection.
US20090181437 Method for producing a conjugated linoleic acid glyceride A method for producing a conjugated linoleic acid glyceride in the form of an ester bond of a conjugated linoleic acid with glycerol, involving reacting a starting material containing a linoleic acid glyceride with a microorganism or an enzyme generated by the microorganism which has a potency to isomerize the linoleic acid glyceride into a conjugated linoleic acid glyceride.
US20080045474 Method for treatment of invasive cells A method for treating metastatic tumor cells of a subject is disclosed. The method comprises administrating to the subject an antisense molecule comprising a nucleotide sequence which is complementary to an RNA sequence of a protease activated receptor (PAR) protein, or an antibody molecule capable of binding to a PAR protein. A method is also described for the treatment of disorders involving the implantation of a placenta in a female subject comprising administrating to the subject the antisense molecule. Also disclosed is the antisense molecule and a pharmaceutical composition comprising it.
US20090088402 Novel agent for inducing apoptosis comprising msx1 or a gene encoding the same as an active ingredient The present invention relates to a novel use of Msx1 protein or a nucleotide encoding the same for inducing apoptosis. The Msx1 of the present invention induces apoptosis through direct interaction with p53 via a homeodomain and such interaction leads to increased stability, and/or nuclear localization of p53 in cells. The Msx1 or homeodomain thereof can be effectively used for the treatment of tumors, in which wild-type p53 protein has lost its function by some mechanism that inactivates p53 proteins.
WO2013183523A1 Method for producing extract from lichen belonging to genus usnea A method for producing an extract from a lichen belonging to the genus Usnea which has a low usnic acid content, said method comprising extracting a lichen belonging to the genus Usnea with an aqueous alcohol solution having an alcohol content of 80 vol% or less.
EP1948662A2 Tricyclic compounds useful as oxytocin receptor agonists Methods for treating and preventing anxiety, anxiety-related disorders, schizophrenia and schizophrenia-related disorders are described herein wherein said methods comprise the administration of oxytocin receptor agonists. of formula 1 , or a pharmaceutically acceptable salt thereof: 1 wherein: G1 is (I) of formula 1 , or a pharmaceutically acceptable salt thereof: 2 wherein: G2 is (II)
US20110257121 Purine nucleoside phosphoramidate Disclosed herein is a compound represented by formula 1 or its hydrate thereof in crystalline or crystal-like form.
US20100016413 Pathotropic targeted gene delivery system for cancer and other disorders Systems for pathotropic (disease-seeking) targeted gene delivery are provided, including viral particles with extremely high titers. In particular, the viral particles are engineered to specifically deliver therapeutic or diagnostic agents to a disease site, such as cancer metastic sites. Personalized dosing regimens are also provided to treat diseases such as cancer efficaciously with reduced adverse side effects.
CN101121696B Metal salt of pyritinol and hydrate of the same The invention belongs to the field of medical technology, relating to a metal salt and the hydrate of the pyritinol, the drug combination containing the pyritinol and the application of the pyritinol in the treatment and virgule or prevention of the cerebrovascular disease; the invention also provides the preparation method. The pharmacological experiments show that the alkaline metal salt of thepyritinol of the invention can reduce the irritation and can be chosen as the substitute of the hydrochloride in the existing market.
US8057807 Use of botulinum toxin therapy for treatment of recalcitrant voiding dysfunction The present invention related to methods for treating neurological-urological conditions. This is accomplished by administration of at least one neurotoxin.
CN103272113A Yinhuang granule for clearing away the lung-heat and preparation method thereof The invention discloses a Yinhuang granule for clearing away the lung-heat and a preparation method thereof. The Yinhuang granule comprises raw materials in parts by weight as follows: 55-65 parts of semen lepidii, 35-40 parts of ephedra or fried ephedra, 40-50 parts of semen armeniacae amarae, 40-50 parts of fritillary bulb, 40-50 parts of folium eriobotryae, 27-32 parts of folium isatidis, 40-50 parts of rhizoma acori graminei, 40-50 parts of dioscorea nipponica makino, 27-32 parts of artemisia rupestris, 40-50 parts of ginkgo leaves, 12-18 parts of schisandra chinensis, 12-18 parts of immature bitter orange, 55-65 parts of gypsum and 12-18 parts of liquorice. Active ingredient content of volatile oil in the prepared Yinhuang granule for clearing away the lung-heat is high, particularly the Yinhuang granule for clearing away the lung-heat has the better curative effect on aspects of clearing lung, eliminating phlegm, clearing lung and eliminating phlegm and the like, and the clinical effect can be played optimally.
EP1689710A1 Indole derivatives for use as chemical uncoupler Novel 3-vinylsulfonyl indole derivatives of formula (I) are chemical uncouplers useful e.g. for treatment of obesity.
CN101766590A Combination for protecting peroxide injury of myocardium The invention provides a combination for protecting peroxide injury of myocardium. The combination comprises the following raw materials (parts by weight of each raw material are shown in brackets): coenzyme Q100 (5 to 50), L-carnitine (10 to 500), and octocosanol (10 to 100). The combination can lessen lipid peroxidation of a myocardium cell membrane and improve the activity of antioxidant enzymes such as SOD, GSH-Px and CAT, thereby protecting the peroxide injury of the myocardium and delaying or eliminating sports fatigue.
WO2014071005A1 Methods and compositions using neuroprotective steroids and thrombolytic agents Described herein are compositions and methods for treating or preventing ischemic injury. In particular, the methods and compositions relate to the use of a neuroprotective steroid, such as a progestogen, such as progesterone or allopregnanolone, and a thrombolytic agent, such as tissue plasminogen activator (tPA). Also described are compositions and methods for reducing the risks of thrombolytic agent treatment using a neuroprotective steroid.
WO2011154772A1 Oral veterinary composition for salmonids, comprising 1-beta-d-ribofuranosyl-1h-1,2,4-triazole-3-carboxamide and use thereof for the treatment of infectious salmon anaemia (isa) in salmonids The invention relates to a novel oral veterinary composition for salmonids, comprising 1-beta-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide and to the use thereof for the treatment of infectious salmon anaemia (ISA) caused by the infectious salmon anaemia or ISA virus in salmonids.
EP2776130A1 A ddr1 antagonist or an inhibitor of ddr1 gene expression for use in the prevention or treatment of crescentic glomerulonephritis The present invention relates to uses, methods and compositions for treating crescentic glomerulonephritis. More specifically, the present invention relates to a DDR1 antagonist or an inhibitor of DDR1 gene expression for the prevention or the treatment of said disease.
US20120022004 Treatment of t-cell mediated diseases The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.
EP1242012A4 Improved transdermal contraceptive delivery system and process A transdermal contraceptive delivery system (TCDS) for fertility control in women is described comprising a backing layer, an adjoining layer of a solid absorption adhesive polymer matrix in which minimum effective daily doses of an estrogen and a progestin are dispersed and released for transdermal absorption. Presently preferred is use of the synthetic estrogen, ethinyl estradiol, and the synthetic progestin, levonorgestrel. Along with these two steroidal contraceptive agents, a combination of several chemical skin permeation enhancing agents, including capric acid, blended at specific weight ratios, ranging from 2.0:1:1:0.8 to 6:1:1:0.8 are homogeneously dispersed in the adhesive polymer matrix. The invention also provides a method of fertility control utilizing the transdermal contraceptive delivery system.
CN1823820A Vitamin and micro element product for prevonting and treating vision injury syndrome due to TV and computer display light and its manufacturing method A medicine used as both medicine and food for preventing and treating vision syndrome caused by computer and television set, such as xerophthalmia, eye strain, blurred vision, hypomnesia, cervical pain, etc, is prepared from vitamins and trace elements. Its preparing process is also disclosed.
EP2037739B1 Benzyl-substituted quinolone m1 receptor positive allosteric modulators The present invention is directed to benzyl-substituted quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of diseases in which the M1 receptor is involved.
EP2112927A2 Method for treatment of overfiltering and leaking blebs with sterile talc The present invention provides a method for treatment of overfiltering and leaking blebs in patients after glaucoma surgery comprising administering to said leaking bleb an effective amount of sterile talc, to thereby seal said leaking bleb and prevent bleb leakage.
CA2269682C Improved pharmaceutical compositions The present invention provides for the inclusion of small amounts of water in oil suspensions of active drugs, such as ceftiofur of formula (II), particularly the hydrochloride salt of ceftiofur. The resulting suspensions have improved resuspendability. Improved resuspendability results in an improved product because less shaking of the suspension is required before dosing.
EP1076651B1 Substituted sulphonyl cyanamides, method for producing same and their use as medicament The invention relates to compounds of formula (I) in which the symbols have the meanings given in the claims. Said compounds are inhibitors of the sodium-dependent bicarbonate/chloride ion exchanger which can be used as medicines for the prophylaxis or treatment of a wide range of diseases, for example the treatment and/or prophylaxis of myocardial infarction, angina pectoris, diseases caused by ischaemia, impaired respiration, cardiac ischaemia, ischaemia of the peripheral and central nervous system and stroke, ischaemia of the peripheral organs and limbs and diseases in which cell proliferation is a primary or secondary cause, in the treatment of shock, during surgical interventions and organ transplants or for preserving and storing transplants to be used in surgical interventions.
WO2011001113A3 Novel 1,2,3,4-tetrahydro-pyrimido(1,2-a)pyrimidin-6-one derivatives, preparation thereof, and pharmaceutical use thereof The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted L-aryl or L-heteroaryl, such that L is a single bond, alkyl, CO, or CO-alk, or L -X, with L being an alkyl and X being O or S; R2 is H or alkyl; R3 is an alkyl optionally substituted by Hal; and R4 is Hou Hal, wherein said materials are in any isomeric form and the salts thereof, to be used as drugs.
CA2412161C Thyroid receptor ligands, pharmaceutical compositions comprising them and their use in the treatment of disorders influenced by thyroid hormones This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor .beta., to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.
US20130028985 Composition and method for treating migraines Disclosed are compositions for treating or preventing migraine headaches and related headaches.
EP1670450B1 Pharmaceutical compositions and method of using levodopa and carbidopa The present invention relates to stable compositions of levodopa and carbidopa, methods of treating patients with these compositions, and methods of preparing these compositions.
EP2063894A2 Formulations containing pyridazine compounds for treating neuroinflammatory diseases The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula (I) are independently hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, sulfate, sulfenyl, sulfinyl, sulfonyl, sulfonate, sulfoxide, silyl, silyloxy, silylalkyl, silylthio, =0, =S, phosphonate, ureido, carboxyl, carbonyl, carbamoyl, or carboxamide; and X is optionally substituted pyrimidinyl or pyridazinyl, an isomer, a pharmaceutically acceptable salt, or derivative thereof. The invention additional relates to compositions comprising the compounds, and methods of using the compounds and compositions for modulation of cellular pathways, for treatment or prevention of inflammatory diseases, for research, drug screening, and therapeutic applications.
US20110065671 Bicyclic heterocycle derivatives and use thereof as gpr119 modulators The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bi-cyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.
WO2014072585A1 Ligneous plant-derived heteropolysaccharides for use in treatment of urologic symptoms and diseases The present invention relates to preventing and/or treating urologic dis- eases and symptoms in humans or domestic animals. The present invention relates also to preventing and/or treating pain in the pelvic area. The invention relates to use of a heteropolysaccharide compositionisolated from ligneous plantsand comprising hemicelluloses, mainly glucomannans, but also xylans and pectic polysaccharides, as well as fractions, subgroups or mixtures of these, as pharmaceutical preparations, food additives and food products.
US20090192180 Alpha-7 Nicotinic Receptor Agonists and Statins In Combination Combinations of α7-nAChR agonists and statins, pharmaceutical compositions containing the same and methods of using the same useful for treatment or prophylaxis of neurological degenerative diseases.
CN101129422A Golden flower mallow health care tablet The invention relates to a health Abelmoschus manihot hard gelatin tablet wherein the weight percents of the active constituent raw material include Abelmoschus manihot seed powder 25-75%, Abelmoschus manihot extract 10-60%, and balancing amount of iso-vitamin C sodium, the content of total flavones is greater than 30mg/100g. The functions of the capsule include improving human body immunity, enhancing constitution, lowering blood fat and blood pressure, improving microcirculation, improving human body's anti-oxidizing ability, and regulating kidney hypofunction.
CN101468974B Semi-synthesizing method for polyenic taxusol The invention discloses a semisynthesis method for polyenic taxusol. The method is to perform condensation reaction between 10-deacetylate baccatin (10-DAB) and synthesized C-13 side chain hydrolysate, open oxazoline rings, inoculate butoxycarbonyl on nitrogen of a side chain, and finally remove protection on a 7 site and a 10 site to obtain the polyenic taxusol.
CN102250190A Oleanolic saponin derivative, preparation method of salt thereof and application of derivative The invention belongs to the technical field of medicaments and provides a 3-O-alpha-L-pyran rhamnose-(1-2)[beta-D-glucopyranose-(1-4)]-alpha-L-pyran arabinose oleanolic saponin derivative, a preparation method of salts thereof as well as application of the derivative in antitumor. The structures of the 3-O-alpha-L-pyran rhamnose-(1-2)[beta-D-glucopyranose-(1-4)]-alpha-L-pyran arabinose oleanolicsaponin derivative and salt thereof are shown in the specification. The 3-O-alpha-L-pyran rhamnose-(1-2)[beta-D-glucopyranose-(1-4)]-alpha-L-pyran arabinose oleanolic saponin derivative and salt thereof can be combined with a pharmaceutically acceptable carrier so as to prepare pharmaceutical compositions and can be used for preparing antitumor medicaments. The medicaments containing the component directive and salt thereof have equivalent or stronger antitumor activity as compared with prototype medicaments and can enhance activities of other antitumor medicaments and reduce the toxic and side effects of the medicaments simultaneously.
CN102091144A Gardenia total polyene composition, preparation method thereof and application thereof to medicaments The invention relates to a gardenia total conjugate polyene composition, a preparation method thereof and application thereof to medicaments, and belongs to the field of the medicaments. According to tests, conjugate polyene compounds in gardenia have synergistic effect. Tumor resistance, hypertension resistance and hyperlipidemia resistance of the gardenia total conjugate polyene composition are higher than those of a control group and a single polyene compound such as crocetin and crocin. The preparation method of the gardenia total conjugate polyene composition is provided.
CN102343022A Beautifying deer fetus particle and preparation method thereof A beautifying deer fetus particle comprises, by weight, 10-70 parts of deer fetus, 10-50 parts of pilose antler, 10-50 parts of deer blood, 10-50 parts of ginseng, 50-150 parts of wolfberry, 10-30 parts of lotus seed, 10-30 parts of almond, 20-100 parts of honey, 30-50 parts of black sesame, 20-50 parts of red dates, 20-50 parts of angelica, 20-50 parts of mythic fungus, 20-50 parts of motherwort, 10-30 parts of pearl powder, 5-30 parts of flos rosae rugosae, 5-10 parts of lotus leaf, 10-30 parts of yam powder and 100-500 parts of brown sugar. The invention also provides a preparation method of the deer fetus particle. The beautifying deer fetus particle of the invention is sweet, tasty, without drug flavour or strange taste and suitable for middle-aged and senior female, can adjust balance of yin and yang in female body, improve physique, endow ruddy complexion and fresh spirit on women, and has functions of beautifying and delaying climacterium.
CN103462962A Application of Incarviatone A in medicaments for treating leukemia The invention relates to an application of Incarviatone A in medicaments for treating leukemia, and belongs to the field of medicines. The invention relates to an application of Incarviatone A in preparation of medicaments for inhibiting leukemia cell proliferation, and an application of Incarviatone A in preparation of medicaments for inducing leukemia cell apoptosis. The Incarviatone A treats the leukemia through inhibiting leukemia cell proliferation and inducing leukemia cell apoptosis. The application of the Incarviatone A in preparation of the medicaments for treating leukemia is made public for the first time, the skeleton type is completely novel, and the Incarviatone A has an unexpectedly strong leukemia cell inhibiting activity.
WO2006060159A1 Method for treating hiv infection through co-administration of tipranavir and gw695634 A method for treating HIV infection through co-administration of tipranavir and GW695634.
WO2011151640A1 Processes for the preparation of dipyridamole The present invention relates to the active pharmaceutical ingredient dipyridamole. In particular, it relates to efficient processes for the preparation of dipyridamole which are amenable to large scale commercial production and provide the required product with improved yield and purity. The present invention also relates to a novel crystallization method for the purification of dipyridamole.
US20110236393 Monoclonal antibody production in b cells and uses therof The presently disclosed subject matter provides methods of inhibiting a host innate response to activator-mediated proliferative signals in a primary B cell. In some embodiments a method is provided for immortalized primary B cells. In some embodiments a method is provided for increasing efficiency of EBV transformation of primary B cells. In some embodiments a method is provided for increasing proliferation of primary B cells in culture. In some embodiments a method is provided for producing a monoclonal antibody. In some embodiments a method is provided for identifying a novel broadly neutralizing antibody having a desired antigen specificity. Also provided are antibodies produced according the methods of the presently disclosed subject matter.
US20110021465 Synergistic composition and method of retarding and ameliorating photo induced retinal damage and cataracts while ameliorating dry eye syndrome A composition and method of retarding and ameliorating eye diseases and injuries is disclosed. The method comprises administering a synergistic mixture of certain carotenoids, including the carotenoid astaxanthin, with phospholipid and triglyceride bound EPA and DHA derived from Krill oil, in which said krill oil contains at least 30% total phospholipids, in a therapeutically effective amount to prevent, retard or treat eye and central nervous system diseases or injuries, such as age-related macular degeneration, cataract, dry eye syndrome due to glandular inflammation and other central nervous system degenerative diseases, photic injury, ischemic diseases, and inflammatory diseases.
EP2167072A1 Use of oleocanthal for treatment of cutaneous inflammation The invention relates to a novel use of oleocanthal. oleocanthal and/or a derivative thereof of general formula (A), where R is H or OH is used for the production of a medicament for topical cutaneous administration for treatment of cutaneous inflammation.
CN102935126A Externally applied medicine for treating burn and scald, and preparation method thereof The invention relates to an externally applied medicine for treating burn and scald. The externally applied medicine is composed of a green leaf paste, garden burnet root, vaseline, metronidazole, ketoconazole, radix notoginseng and musk. The proportion range of each raw material drug is as follows: 15-30 g of green leaf paste, 10-15 g of garden burnet root, 10-25 g of vaseline, 20-30 g of metronidazole, 20-30 g of ketoconazole, 5-8 g of radix notoginseng and 5-8 g of musk. The externally applied medicine can improve anti-infection capability, inhibits exudation, relieves pains and heals the burn rapidly.
US20110091407 Polymer derived from linear polyethylenimine for gene transfer The invention relates to a static copolymer of linear polyethylenimine that comprises two monomer units of the following formulas I and II, in which R1 is a hydrogen atom or a C1-C6 alkyl radical, R2 is a hydrogen atom, a C1-C6 alkyl, aryl or aralkyl group, wherein the alkyl group is a C1-C6 one, n is a number between 1 and 99% of the total monomers, m is a number between 1 and 99% of the total monomers, and advantageously m+n=100%. The invention also relates to complexes of this copolymer with a nucleic acid, and to the use thereof in in vivo, in vitro or ex vivo gene transfection.
CA2645982A1 Use of ave5026 for minimizing the incidence of bleedings during an antithrombotic treatment The invention relates to the use of AVE5026 for minimizing the incidence of bleedings during an antithrombotic treatment.
CN102772777A Medicine for treating infantile pneumonia and preparation method thereof The invention discloses a medicine for treating infantile pneumonia and a preparation method thereof. The medicine is mainly prepared from ginseng, honeysuckle, radix salviae miltiorrhizae, bamboo leaf, prepared radix licorice, rhizoma zingiberis, fructus forsythiae and monkshood which are proportioned according to a certain weight ratio, the medicine disclosed by the invention has excellent effect on the symptoms of eupyrexia or hectic fever, obvious asthma and slight sweating or hypohidrosis, and the medicine has quick-acting treatment effect on infantile pneumonia without relapse and the treatment course is short.
EP1359979B1 Anti cancer combination of substituted pyrroles and paclitaxel Disclosed is a process of treating a patient suffering from cancer. The process compriese administering to a patient over a period of up to about 15 days a first component and a second component. The first component consists of a pharmaceutical composition containin as an active ingreadient a compound of formula (I) or a pharmaceutically acceptable salt or ester of said compound. the second ocmponenet consists of a n injection solution containing as an active ingredient paclitaxel. The amount of each componet in the combination is such that the combination is therapeutically effective. The components are administered concomitantly or sequentially ina three week to four week treatment cycle for as long as the tumor remains under control and the patient tolerates the regimen.
US20080021015 Use as medicine of a compound restoring active principles in vivo A method for delivering at least an active principal A to a human or animal, by administering, in vivo, an active compound of general formula A′ V′
CN101690718A Carteolol hydrochloride pellets, preparation method thereof and preparation thereof The invention discloses a carteolol hydrochloride pellets, a preparation method thereof and a preparation thereof. The pellets comprise the following components in part by weight: 30 to 50 parts of carteolol, 60 to 120 parts of filler and 0 to parts of lubricant and have the advantages of high bioavailability, small local irritation, even medicament absorbing speed and the like. The preparation method adopts an extrusion spheronization method or a centrifugation granulation method, has simple operation, easy controlled quality and low cost, and is applicable to industrial production; and the prepared pellets have narrow granularity distribution range, good roundness and smooth surface, can be quickly disintegrated and dispersed in the stomach, can be further made into coated pellets, pellet tablets or pellet capsules to improve the stability of the carteolol and effectively cover the bitter taste of the carteolol, are convenient in carrying and taking, improvethe medicament compliance for patients and have wide application prospect in disease treatment fields, such as hypertension, angina, arrhythmia, cardioneurosis, infants with tetralogy of fallot and the like.
US20100098768 Method of neuroprotection from oxidant injury using metal oxide nanoparticles A metal oxide nanoparticle composition including a cerium oxide nanoparticle and a metal adapted to enhance the neuroprotective activity of the cerium oxide nanoparticle. The metal can include noble metals such as platinum, and rare earth metals such as gadolinium, samarium, titanium, yttrium, zirconium, and a combination thereof Another metal oxide nanoparticle composition including a cerium oxide nanoparticle and a surface modifier, such as polyethylene oxide, polyethylene imine, dextran, polylactic acid, chitosan, alginate, and a combination thereof is provided. A method of using the metal oxide nanoparticle compositions as neuroprotective agents for the inactivation of reactive oxygen species in nervous tissues is also provided. More specifically, a neuroprotective method using the metal oxides such as ceria, yttria, or mixed ceria and yttria (or any of the other referenced metal oxide nanoparticle compositions) before, during, or after an ischemic event.
CA2224635C Pyridine derivatives, process for preparing the same, and intermediate therefor The present invention is directed to a pyridine derivative of the formula (I):(see formula I) wherein A is group of the following formulae:(see formula II) (R1 and R2 are each H, or protected or unprotected OH, R31, R41 and R42 are protected or unprotected hydroxymethyl, R32 is H, lower alkyl, or protected or unprotected hydroxymethyl, R33 is substituted or unsubstituted lower alkyl, and the dotted line means the presence or absence of a double bond), R5 and R6 are H, or protected or unprotected amino, or both combine together with the adjacent nitrogen to form substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof. These compounds showing excellent bronchoconstriction inhibitory activity and/or airway anti-inflammatory activity, and are useful in the prophylaxis or treatment of asthma.
US20100056560 Use for treating obesity and diabetes Disclosed herein is the use of a composition, containing isoflavone-containing soybean extract, L-carnitine, caffeine and arginine as active ingredients, for the treatment of obesity and diabetes. The disclosed composition contains isoflavone-containing soybean extract, carnitine, caffeine and arginine in the form of a mixture, and thus shows not only the effect of promoting lipolysis and fat burning, but also anti-obesity and anti-diabetic effects by increasing the expressions of adiponectin and Glut4 genes to restore insulin sensitivity.
WO2011020822A1 Substituted (thiazolyl-carbonyl)imidazolidinones and use thereof for treating retroviral diseases The present invention relates to novel substituted (thiazolyl-carbonyl)imidazolidinones, to a method for the production thereof, to the use thereof for the treatment and/or prophylaxis of diseases, and to the use thereof for producing pharmaceuticals for the treatment and/or prophylaxis of diseases, in particular retroviral diseases, in humans and/or animals.
CA2362625C Frozen chlorine dioxide-containing composition and methods related thereto A frozen chlorine dioxide-containing composition comprising a metal chlorite and a protic acid in a frozen aqueous matrix made by freezing a substantially chloride dioxide-free aqueous solution comprising a metal chlorite at a concentration ranging from about 0.0005% to about 0.5% by weight and a protic acid at a concentration sufficient to lower the pH of the aqueous solution to a value of about 1.8 to about 5Ø The frozen chlorine dioxide-containing composition has a chlorine dioxide concentration of more than about 3 ppm, while the aqueous solution prior to freezing has a chlorine dioxide concentration less than about 3 ppm. The frozen chlorine dioxide-containing composition is used to disinfect substrates by contacting the same with the frozen chlorine dioxide-containing composition. Suitable substrates include food intended for human or animal consumption, such as meat, fish and poultry.
US20080242703 Pharmaceutical compositions for the treatment of hearing loss The present invention provides a pharmaceutical composition for the treatment of hearing loss. The pharmaceutical composition of the present invention comprises a proton pump inhibitor (PPI), and is useful to decreasing acute or chronic hearing loss of patients related to the mutation or degenerative dysfunction of SLC26A4 gene.
WO2013088191A1 Antagonist of the fibroblast growth factor receptor 3 (fgfr3) for use in the treatment or the prevention of skeletal disorders linked with abnormal activation of fgfr3 The present invention relates to the treatment or prevention of skeletal disorders, in particular skeletal diseases, developed by patients that display abnormal increased activation of the fibroblast growth factor receptor 3 (FGFR3), in particular by expression of a constitutively activated mutant of FGFR3.
CN103127101A Application of 8-diethyl malonate berberine in preparation of antitumor drug The invention belongs to the chemical industry field and the medicine field, and relates to an application of 8-diethyl malonate berberine in preparation of antitumor drugs. The invention provides the application of 8-diethyl malonate berberine in preparation of antitumor drugs, and the tumor cells comprise leukemia cells and pancreas cancer cells. The 8-diethyl malonate berberine belongs to a natural product, has little toxic and side effect, high bioavailability, and stable properties, and has clinical application value. The micromolecular compound of the invention can be developed as a new antitumor drug or its auxiliary component, has obvious tumor suppression effect, is green and environment-friendly, and provides a new approach and means for treating and curing tumors.
EP1715877A1 Compositions and methods for reducing cholesterol comprising guggul and beta-glucan and/or plant sterols There are disclosed compositions comprising guggul and at least one of 1, 3:1, 4 - beta - glucan or a beta-sitosterol-containing sterol mixture. The compositions are preferably suitable for reducing cholesterol level. Also disclosed are food and beverage compositions comprising the guggul-containing compositions, that are preferably suitable for reducing cholesterol level. There is also disclosed a method for reducing cholesterol level comprising administering to a human or animal, an effective amount of the guggul-containing compositions, or a food or beverage composition that comprises the guggul-containing compositions.
EP2212299A1 Piperazinyl-sulfonamide derivatives useful in the treatment of gpr38 receptor mediated diseases The present invention relates to novel motilin agonists of formula (IA), processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
CN101244133A Rheumatism-treating medical liquor and preparation thereof The invention relates to a medical wine for treating rheumatism as well as the preparation method. The preparation method comprises the following steps: first, use mineral water to respectively rinse 50 to 70g safflower, 50 to 70g angelica sinensis, 50 to 70g rhizoma ligustici wallichii, 30 to 50g cortex periplocae, 60 to 80g pawpaw and 110 to 130g giant knotweed; next, steep the active pharmaceutical ingredients into 900 to 1100ml broomcorn distilled liquor with 35 percent to 45 percent as the concentration for 25 to 35days; then filter the residue and get the extractant to put in the vessel; finally, seal and store after sterilization. The medical wine has the advantages of convenient collection of the raw materials, low price, totally natural materials, no poison and side effect and simple preparation. The medical wine is suitable for various rheumatisms and also for numbness of limbs, sciatica, cervical spondylosis and hyperosteogeny.
WO2009000132A1 Immediate release effervescent-formulation and preparing process thereof An immediate release effervescent-formulation in which unpleasant taste of drug is masked, comprising effervescent matrix, active compound coated with stomach-soluble polymers, and process for their preparation.
US7803954 Mandelic acid derivatives and their use as thrombin inhibitors There is provided a compound of formula (I) wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g., thrombosis) or as anticoagulants.
US20110077287 Pharmaceutical composition containing a stabilised mrna optimised for translation in its coding regions The present invention relates to a pharmaceutical composition containing an mRNA that is stabilised by sequence modifications in the translated region and is optimised for the translation. The pharmaceutical composition according to the invention is particularly suitable as an inoculating agent as well as a therapeutic agent for tissue regeneration. In addition a process is described for determining sequence modifications that serve for the stabilisation and translation optimisation of mRNA.
CN102391260A 3-ketone-6-substituted-benzofuran compound as well as preparation method and application thereof The invention relates to a 3-ketone-6-substituted-benzofuran compound as well as a preparation method and application thereof. The 3-ketone-6-substituted-benzofuran compound has the following structural formula: the preferable 3-ketone-6-substituted-benzofuran compound can be used for preparing medicament capable of inhibiting the biological activity of the microorganism. Compared with the prior art, the 3-ketone-6-substituted-benzofuran compound takes 3-ketone substituent group benzofuran as a aromatic ring center; (5-methyl-2-phenyloxazole-4-yl) ethyoxyl is introduced into the 6th position of the benzofuran to obtain a novel compound; the preparation method of the compound is built and optimized; the prepared novel compound is subjected to a bacteriostat screening experiment; a primary in-vitro bacteriostat experiment confirms that the parts of prepared new compounds have excellent broad spectrum bacteriostasis activity; and the 3-ketone-6-substituted-benzofuran compound can be used for preparing the novel antibacterial medicament.
WO2009101182A1 Use of etonogestrel for benign prostate hyperplasia (bph). The invention provides for the use of tonogestrel for a treatment of an individual having benign prostate hyperplasia, preferably with a spray or solution into the oral cavity of the individual in need of the treatment. The treatment can be for a period of a duration in the range of from 2 to 12 weeks in which a daily dose of etonogestrel in an amount per dose in the range of from 0.07 mg to 0.3 mg is administered to the individual followed by a period without administering etonogestrel for a duration in the range of from 1 month to 6 months.
WO2006077816A1 Imidazopyridine derivative The invention relates to a novel imidazo[4,5-b]pyridine derivative compound represented by the formula (I) and a pharmaceutically acceptable salt thereof. The invention also relates to a method of producing the compound. The invention further relates to a pharmaceutical composition comprising the compound. The compound has a growth inhibiting activity against a cancer cell, and further, the activity is distinct from a growth inhibiting activity against a normal cell. Therefore, it is useful as a novel anticancer agent.
US20110294901 Finely pulverized pharmaceutical composition An objective of the present invention is to provide a composition that has improved oral absorption and comprises a slightly soluble drug, and to provide a process for producing the same. According to the present invention, there is provided a finely pulverized composition comprising a slightly soluble drug such as 22β-methoxyolean-12-ene-3β, 24(4β)-diol and a hydrophilic surfactant. According to the present invention, there is also provided a process for producing the finely pulverized composition according to the present invention, characterized in that, after the dispersion of a slightly soluble drug and a hydrophilic surfactant in a solvent, the dispersion is pulverized with a high-pressure homogenizer.
EP1219632B1 Steroids, their preparation, pharmaceutical compositions thereof and uses of the compounds The present invention relates to steroids of general formula (I), wherein R1 is cyclohexyl, suberyl, R2 is hydrogen or C¿1?-C6-alkyl, R?3¿ is hydrogen, C¿1?-C6-alkyl or hydroxymethyl, R?4¿ is hydrogen or hydroxymethene, or pharmaceutically acceptable salts thereof, to processes for their preparation, to pharmaceutical compositions containing the compounds as active components and to uses of the compounds and pharmaceutical compositions for the preparation of a medicine for treatment of progestogen-dependent related disorders.
US20080090789 Tigecycline crystalline forms and processes for preparation thereof The present invention relates to solid crystalline Tigecycline, and crystalline forms thereof.
WO2012168720A1 MATERIALS AND METHODS FOR TREATING ESTROGEN RECEPTOR α (ER) POSITIVE CANCER Experiments described herein in which the genetic dependency on ADCK2 is shown in endocrine receptor positive cancer. Accordingly, the use of ACDK2 inhibitors for treating individuals having estrogen receptor α (ER) positive cancers, such as ER positive breast cancer, ovarian cancer, prostate cancer or endometrial cancer, are disclosed.
US20100331273 Self-assembling complex for targeting chemical agents to cells The present invention relates to a complex that can be injected into the body to hone in on target cells to deliver molecules. In one embodiment, the invention provides a drug delivery system that includes components that self-assemble into one targeted conjugate. In another embodiment, the invention includes a targeted carrier protein and a nucleic acid sequence non-covalently linked to one or more drugs.
EP2628733A1 Acylbenzene derivative Provided are compounds having an excellent hypoglycemic action and a β cell- or pancreas-protecting action or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
US20110034472 Novel Compounds for Treatment of Cancer and Disorders Associated With Angiogenesis Function Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression.
US20110166095 Cancer platinum resistance detection and sensitization method The phosphorylation status of the BAD protein is a determinant of ovarian cancer cell responsiveness to platinum chemotherapy. Indirect manipulation of BAD phosphorylation status influences cisplatin sensitivity. BAD phosphorylation represents a biomarker that predicts platinum sensitivity and is a therapeutic target to increase platinum sensitivity. The methods employ phospho-specific antibody against a particular amino acid residue or site. Phospho-specific protein characterization methods include immunohistochemical (IHC), flow cytometric, immunofluorescent, capture-and-detection, or reversed phase assay.
CN101264103A Application of native copper native copper microbial extracting liquid in preparing medicaments for treating bone fracture The invention relates to the application of microbial leaching solution of natural-copper in preparing drugs treating fracture. The leaching solution of natural-copper is prepared according to the bacteria processing method publicized by 2006102000675 of Chinese invention patent application. The microbial leaching solution of natural-copper has the advantages that: leaching solution of natural-copper has obvious result in promoting healing of the fracture with small amount; because leaching solution of natural-copper is soluble and can be easily made into each formulation singly or jointly with other drug compatibility or accessories accepted pharmaceutically. The formulation has a plurality types comprising suppository, medical pill, granule, film agent, microcapsules, dropping pill, aerosol preparation, medicinal wine, syrup, oral liquid/solution, injection or injection of injection powder and other formulations.
CN1939276A Oral preparation containing paracillin and its making method An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains piperacillin. Its preparing process is also disclosed.
WO2014033343A1 Beta-3 adrenoceptor agonists for the treatment of pulmonary hypertension The invention relates to the use of selective agonists of beta-3 adrenergic receptors for the treatment and/or prevention of pulmonary hypertension.
WO2013078392A1 Methods and compositions involving induced senescent cells for cancer treatment Disclosed are cancer vaccines comprising senescent cells and methods of using and preparing the vaccines.
WO2006030299A1 Processes for the preparation of polymorphs of efavirenz The invention relates to processes for the preparation of polymorphic forms of efavirenz. More particularly, it relates to the preparation of Form I and Form II of efavirenz. The invention also relates to pharmaceutical compositions that include the Form I of efavirenz and use of said compositions for treatment of HIV-1 infections in combination with other antiretroviral agents.
CN103102360A Alanine copper complex as well as preparation method and application thereof The invention provides an alanine copper complex as well as a preparation method and an application thereof. The alanine copper complex has coordination of lactamine and copper ions and can also contain other organic micro-molecular ligands. The preparation method of the alanine copper complex comprises the following steps of: putting lactamine, a cupric salt, alkali and other organic micro-molecular ligands into a solvent, and stirring for reaction to obtain the alanine copper complex. The alanine copper complex is easily available in synthetic raw material and low in cost, and the product is separated out in the form of crystal and is high in purity and yield; the alanine copper complex can stably exist in a natural state and has high water solubility and fat solubility; and moreover, the alanine copper complex has a good function of inhibiting a variety of cancer cells such as cells of lung cancer, stomach cancer, liver cancer, colonic gland, leukemia, nasopharyngeal darcinoma and the like, and is wide in action spectrum and application range.
US7001904 Guanidine derivatives quinazoline and quinoline for use in the treatment of autoimmune diseases The invention concerns quinazoline and quinoline derivatives of Formula (I) wherein Q1 includes a quinazoline or quinoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2, R3 and R5 is hydrogen or (1-6C)alkyl, provides that one of the parts of groups R2 and R4 together, R3 and R4 together and R5 and R4 together forms a bond; R6 is an optionally substituted group selected from (2-6C) alkenyl, (2-6C) alkynyl, (3-7C)cycloalkyl and (3-7C) cycloalkenyl, or R6 is a substituted (1-6C) alkyl group; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.
CN101231233A Method for controlling release velocity of fluorescent probe molecule in emulsions A method for controlling the speed of releasing the fluorescent probe molecules in the latex emulsion belongs to the material controlled release technical field. The art is as follows: a fluorescent probe molecule water solution or a polymer-fluorescent probe molecule water solution taken as the water phase is added into a mineral oil phase containing a polylol non-ionic surface promoting agent, the volume ratio of the polylol non-ionic surface promoting agent to the mineral oil ranges from 1:19 to 1:10, the solution is evenly stirred at a rotating speed of 8000 to 12000 turns per minute under 273 to 298 K for 1 to 5 minutes to get a water-in-oil latex emulsion, a 0.8 milliliters of water solution containing two to four percent of polyoxyethylene sorbitan laurate is added into to the prepared water-in-oil latex emulsion to be emulsionized for the second time for 2 to 5 minutes to obtain the water-in-oil or oil-in-water latex double emulsion. The sample is analyzed by a fluorescent energetic cell sorter and the release speed of the fluorescent probe molecules is calculated by a formula. The invention has the advantages of high speed, high efficiency, directness and accuracy.
CN103340853A Compound 18-amino acid injection containing little amount of antioxidant and preparation method thereof The invention relates to a compound 18-amino acid injection containing a little amount of antioxidant and a preparation method thereof. The injection contains 0.0005w/v% to 0.005w/v% of sodium hydrogen sulfite or sodium metabisulfite or mixture which is compounded with 18 kinds of amino acids and water for injection, wherein the content of dissolved oxygen in the injection is not greater than 0.1ppm (parts per million). The preparation method comprises the following steps of: 1) preparing: putting 18 kinds of compound amino acids, the sodium hydrogen sulfite or the sodium metabisulfiteor or the mixture into a tank by filling nitrogen ceaselessly under the conditions that content of oxygen in the tank is lower than 0.1% and the content of the dissolved oxygen contained in the injection is not greater than 0.1ppm; 2) filling and sealing; and 3) sterilizing. By optimizing a production process, the oxygen content of a medicine liquid and the oxygen content of a headspace are reduced fundamentally, so that the content of the sodium bisulfite/the sodium metabisulfite which is added for ensuring that the medicine liquid is not oxidized is reduced. Thus, the compound amino acid injection which can be well tolerated by a patient is produced, namely, the safety of the injection is improved. Therefore, the phenomenon that a sufficient dose of the injection cannot be accepted by the patient because the patient is worry about toxic and side effects is avoided. As a result, the injection provided by the invention has the great significance for guaranteeing the living and the life quality of the patient.
US20080076743 osteoarthritis; administered once daily for at least about two weeks The present invention refers to the treatment of a rheumatic disease and/or osteoarthritis by administering a delayed-release dosage form of a glucocorticoid to a subject in need thereof.
WO2007103727A3 Triterpene derivatives for the treatment of cancer and inflammatory disease by inhibition of nf-kb The present invention relates to the use of triterpenes of the formula (I): which are inhibitors of nuclear factor kappa B (NF-KB for use in the treatment of inflammatory diseases and for cancers susceptible to an NF-KB inhibitor. The present invention also relates to compounds and methods useful to inhibit cell proliferation and for the induction of apoptosis.
US20100285124 Tetrahydrocyclopenta[c]acridine derivatives as kinase inhibitors and biological The invention relates to kinase inhibitors of the formula (I) in which —R1 to R4=H; ether or polyether, amino; NO2; NH— carbamate; NH—CO—R, with R such as defined above; N3 and derivatives thereof of the 1,2,3-triazole type; —R5=—OH; halogen; —OR with R such as defined above; OH-carbamate; OH-carbonate; NH2, NH-carbamate; NH—CO—R, with R such as defined above; N3 and derivatives thereof of the 1,2,3-triazole type; N(R9, R10); —R5′=H or a C1-C12 alkyl, —R6=H; R; (R or R′)3—Si, with R such as defined above; optionally substituted aryl, heteroaryl; halogen (iodine); alkynyl; —R7 and R8=H, C1-C12 alkyl; —R9 and R10=H, R (or R′) such as defined above. These compounds can be used as kinase inhibitors in particular for treating cancer.
CN1969929A Dry coating sustained-release tablet for treating arthritis and preparation process thereof The invention discloses a kind of dry dressed controlled release tablets for treating arthritis which comprises medicinal cores and dry coating sheet, wherein the dry coating sheet comprises slow release matrix material 110-150 parts, hole-making agent 100-120 parts, right amount of binding agent and magnesium stearate. The medicinal cores comprise Tripterygium wilfordii glycosides 20-30 parts, crumbling agent 10-20 parts, bonding agent 20-30 parts, thinning agent 30-40 parts, and right amount of magnesium stearate.
CN1977795A Use of total cistanchis glycoside for inhibiting skin pigment deposition and whitening The present invention relates to a new application of cistanche total gluooside. The tests show that the cistanche total glucoside has obvious effect for reducing activity of tyrosinase, so that the cistanche total glucoside has the functions of inhibiting cutaneous pigmentation and whitening and beautifying face.
EP0784430B1 Method for reducing unwanted cellular adhesions A conjugate comprising a drug which has an inhibitory effect on cellular adhesion and a lipophilic cell binding agent, when applied to a compromised site, e.g., due to surgical intervention, injury, chemotherapy, disease or inflammation, is effective in reducing unwanted adhesion formation.
CN103656297A Chinese drug agentia for treating tympanitis and preparation method of Chinese drug agentia The invention discloses a Chinese drug agentia for treating tympanitis and a preparation method of the Chinese drug agentia. The Chinese drug agentia comprises the following drug substances in parts by weight: 5-8 parts of roots of Indian abutilon, 9-13 parts of common cyanotis roots, 5-8 parts of coromadel coast falsemallow herb, 3-8 parts of auricled hedyotis herb, 10-20 parts of honeysuckle, 6-9 parts of prepared rehmannia roots, 12-20 parts of fructus momordicae, 6-12 parts of borneol, 5-8 parts of finless eel blood, 10-14 parts of cicada ecdysis and 5-8 parts of Chinese francolin claw. Compared with the prior art, the Chinese drug agentia for treating tympanitis and the preparation method of the Chinese drug agentia have the following advantages: on one hand, the efficacy is significant, and the patient resistance is enhanced; the price is low, the Chinese drug agentia has no toxic or side effects, and the preparation method is simple and convenient and suitable for clinical application; on the other hand, as an oral drug, the Chinese drug agentia is more convenient to use than external medicine, and is not easy to relapse.
WO2006134970A1 Coenzyme q10-containing water-soluble composition and process for production thereof Disclosed is a coenzyme Q10-containing water-soluble composition which can retain a stable emulsified state for a prolonged time of period at a temperature ranging from a low temperature to ambient temperature and has a high bioavailability including the capability of effective supply. A coenzyme Q10-containing water-soluble composition comprising coenzyme Q10, a hydrophilic polyglycerin fatty acid ester, a lipophilic sucrose fatty acid ester and an aqueous phase; a process for producing the composition; a coenzyme Q10-containing water-soluble dried powder which is produced by drying the coenzyme Q10-containing water-soluble composition; and a food, functional food, beverage, pharmaceutical preparation, medicated cosmetic, cosmetic or animal feed prepared using the coenzyme Q10-containing water-soluble composition or coenzyme Q10-containing water-soluble dried powder.
CN103006579A Application of salvianolic acid A lyophilized powder injection in preparation of drugs for protecting cerebrovascular endothelial cells The invention relates to application of salvianolic acid A lyophilized powder injection in preparation of drugs for protecting cerebrovascular endothelial cells. The salvianolic acid A lyophilized powder injection comprises, by weight, 20-60g of salvianolic acid A, 20-60g of filling agent, and an antioxidant accounting for 0.02%-0.1% of the total amount of the finished product.
WO2006138418A3 Improvement of cognitive performance with sirtuin activators Provided herein are methods and compositions for enhancing the cognitive performance of a subject in need thereof. A method may include administering to a subject an agent that increases the level of protein or activity of a sirtuin, such as SIRTl.
EP1682162B1 Use of prickly pear (opuntia) for the preparation of a medicament for the treatment of depressions The invention relates to the use of opuntia, plant parts thereof, and/or extracts or other preparations produced therefrom for the treatment of depressive moods and diseases or other affective disorders which can be influenced by antidepressants, such as anxiety and panic disorders, bipolar depressions, somatization disorders, premenstrual syndrome, and precursors of such diseases.
US20050003013 Controlled rate and duration of release; degradable gel with controlled saturated moisture content A drug is provided comprising of a degradable gel with a saturated moisture content not exceeding 98 wt. % and a functional material, and which permits control of the rate of release of the functional material and performs controlled-release of the functional material over a prolonged period of time, and wherein the gel itself decomposes and dissipates upon completion of release of the functional material.
WO2013151923A1 Pyrimidinone carboxamides as inhibitors of endothelial lipase The present invention provides compounds of Formula (I): (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
WO2006082354A1 Azacyclic compounds as inhibitors of sensory neurone specific channels ( sns ) Compounds of the formula (I) , and pharmaceutically acceptable salts thereof , are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents. wherein: - Ar represents a phenyl ring or a 5 - to 6- membered heteroaryl group; - m is 1 , 2 or 3 .
WO2006074293A3 Bicyclic dihydropyrimidines as eg5 inhibitors The present invention provides compounds having formula (I): (I) and pharmaceutically acceptable derivatives thereof; as described generally and in subclasses herein, which compounds are useful as kinesin inhibitors (e.g., Eg5 inhibitors), and thus are useful, for example, for the treatment of proliferative disorders e.g., cancer. The invention additionally provides methods for preparing compounds of the invention, compositions comprising them, and methods for the use thereof in the treatment of various disorders where Eg5 is involved. In certain embodiments, the present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.
WO2006042406A1 Method for modification of ϝ-secretase activity through inhibition of fkbp13 The present invention provides a method for modifying y-secretase activity in a cell or in an organism by destabilizing presenilin through inhibition of Fkbp13. Inhibition of Fkbp13 de-stabilizes presenilin and prevents formation of a functional y-secretase complex thus decreasing y-secretase activity and concomitantly decreasing production of amyloid-ß peptides. The invention also provides methods for identifying agents which function to inhibit Fkbp13.
US20050124594 Prophylactic treatment of eyes as having high risk of developing choroidal neovascularisation in macular degerneration by injecting an antiinflammatory steroid, e.g., triamcinolone acetonide, into the vitreous; occult and classic neovascularisation; mixture with antibiotic or angiogenesis inhibitors This invention relates to the prophylaxis of choroidal neovascularisation in macular degeneration by the introduction of a suitable anti-inflammatory agent into the vitreous. In particular, it relates to the prophylaxis of neovascularisation with an anti-inflammatory steroid, such as an 11-substituted 16 alpha, 17 alpha-substituted methylenedioxy steroid of formula (I) wherein (a) is (b), (c), (d), (e), (f), (g), (h), (i), (j), (k) or (l); R1 and R2 are hydrogen or alkyl; -Ca-Cb- is —CH2—CH2—, —CH═CH—, (m) or (n); R3 is methyl, hydroxymethyl or alkylcarbonyloxymethyl, methylaminoalkylenecarbonyloxymethyl, or phenylaminoalkylenecarbonyloxymethyl; R4 is alkanoyl; and X is halogen in eyes which have been identified as having a high risk of developing choroidal neovascularisation. More particularly, it relates to prophylaxis with triamcinolone acetonide, (compound II).
CN102008445A Amoxicillin soluble powder as well as preparation method and application thereof The invention provides an amoxicillin soluble powder as well as a preparation method and application thereof, which can solve the problem in the prior art that amoxicillin has low solubility in water and has big possibility of deteriorating in water. The invention adopts the following technical scheme: the amoxicillin soluble powder comprises the following components in percentage by weight: 1-50 wt% of amoxicillin and 50-99 wt% of polyethylene glycol. The invention also provides the preparation method and application of the amoxicillin soluble powder. With respect to the amoxicillin soluble powder prepared by the invention, the solubility of amoxicillin in water is increased and the stability of amoxicillin in water is improved.
WO2014044025A1 Pyrimidineamide derivative and preparation method and use thereof Provided are a pyrimidineamide derivative as represented by general formula (I), pharmaceutically acceptable salt thereof, and stereoisomer thereof or solvent compound thereof, wherein X, Y, A, R1 and R2 are as defined in the specification; also provided are a preparation method of the compounds, pharmaceutical composition containing the compounds, and uses of the compounds in the preparation of drugs for treating and/or preventing syk-mediated signal-path-related diseases.
WO2013013351A1 Immediate release-sustained release osmotic pump perparation of compund methoxyphenamine Disclosed is animmediate release-sustained release osmotic pump tablet comprising methoxyphenamine or its hydrochloride, noscapine, aminophylline, chlorphenamine maleate. The tablet comprises two drug-release parts，andone is immediate release part comprising 1-70% of active ingredient coated on the surface of the osmotic pump tablet，whichmake drugs immediately release when the tablet gets into the stomach；while the other is sustained release part comprising 30-99% of active ingredient which is in the inside of the osmotic pump tablet. The sustained release part can continually release drug for 8-24 hours.
WO2009063202A3 Use of crth2 antagonist compounds The invention relates to compounds of general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein for the treatment of allergic conditions, wherein the treatment is by pulsed therapy which comprises a first period during which the compound is administered to the patient and a second period of at least seven days during which the compound is administered to the patient in a reduced amount.
US20100197611 Alternative agent with vitamin d-like activity and an improving agent for intestinal function The present invention relates to an alternative agent with vitamin D-like activity or an improving agent for age-related depression of intestinal function, comprising a sugar-phosphate ester or a salt thereof, as an active ingredient.
US8003676 1,3,4-oxadiazole derivatives as DGAT1 inhibitors Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein: n is 1, 2 or 3 and each R is independently selected from fluoro, chloro, cyano, methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy and difluoromethoxy; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
CN102850422A Dexamethasone small-molecular hydrogel drug delivery system and preparation method thereof The invention relates to a dexamethasone small-molecular hydrogel drug delivery system and a preparation method thereof. According to the invention, dexamethasone is subjected to derivatization by using 1,4-succinic anhydride or glutaric anhydride, such that a dexamethasone prodrug is formed. Through pH value regulation, the prodrug is subjected to auto-hydrolysis, such that dexamethasone drug molecules are released; the molecules are subjected to self-assembly spontaneously, such that the small-molecular hydrogel is formed. Specifically, dexamethasone 21 hydroxyl site derivatization is achieved by using 1,4-succinic anhydride (glutaric anhydride), such that gel-forming precursor molecules are obtained. The precursor molecules have good solubility, high drug load, and simple components. Through auto-hydrolysis, dexamethasone drug molecules can be released, and can be spontaneously self-assembled into the hydrogel. The process does not need to be driven by any chemical reagent. According to the system, drug molecules and derivatized drug are adopted as carriers, such that other carriers are not needed. Therefore, the dexamethasone novel delivery system provided by the invention assists in improving solubility and drug load of dexamethasone in water, and is potential to be developed into a novel preparation form of dexamethasone.
US20090124691 Inhibitor of increase in postprandial blood insulin level The present invention provides an agent for inhibiting a postprandial increase in blood insulin level, wherein the agent containing a monoacylglycerol as an active ingredient. An agent of the invention for inhibiting a postprandial increase in blood insulin level contains a monoacylglycerol as an active ingredient.
CA2247467C Use of piperine as a bioavailability enhancer Compositions and methods for the improvement of gastrointestinal absorption and systemic utilization of nutrients and nutritional supplements, wherein the compositions comprise a minimum of 98 % of pure alkaloid piperine. The method comprises oral, topical, or parenteral administration of the compositions of the invention. A new process for the extraction and purification of piperine is also disclosed.
US7217698 Tetraacylated N-cyclopropylcarbonylmannosamines; treating Alzheimer's and Parkinson's disease The present invention relates to the use of peracylated N-acyl-mannosamine derivatives for the preparation of a medicament for stimulating neurite growth.
WO2007072800A1 Photosensitizing compound Disclosed is a photosensitizing compound represented by the formula (I): (I) wherein R1 represents a hydrogen atom, a C1-12 alkyl group or a C1-12 alkoxy group; R2 represents a C1-12 alkyl group or a C1-12 alkoxy group; R3, R4, R5, R6, R7 and R8 independently represent a hydrogen or halogen atom; and R9 represents a monovalent group capable of being cleaved by contacting with an enzyme or a reactive oxygen species. The compound of the formula (I) can serve as a photosensitizer when the group R9 is cleaved out from the compound by contacting with an enzyme or a reactive oxygen species expressed in a target cell, and therefore is useful as a PDT pharmaceutical which can kill the target cell selectively by irradiation with excited light.
US20060088530 Administering lyposomes of photosensitive receptors or ligands targeted to specific tissues, exposure to light causing destruction of bound tissues; treatment of eye neovascular disease due to macular degeneration, diabetes This invention discloses methods, kits, and instructions to treat neovasculature diseases of the eye through the administration of a targeted photosensitizing agent and subsequent exposure to light of specific wavelength sufficient to photoactivate photosensitizing agent. The photosensitizing agent is bound to a composition that mediates site specific delivery to a neovasculature target tissue of a therapeutically effective amount of a photosensitizing agent that is activated by a relatively low fluence rate of light over a prolonged period of time. Diseases treatable under this invention, include: diabetic retinopathy; macular degeneration; and malignant uveal melanomas.
WO2011112875A2 Foamable formulation The present invention provides DMSO-containing foamable formulations, methods for preparation, and methods of treatment. The formulations can provide good permeability and bioavailability at the target site. Preferably, the formulations are useful for treating osteoarthritis. In one embodiment, the invention provides a foamable formulation for topical use, said formulation comprising DMSO, polyalkylene glycol alkyl ether, an active agent, a monohydric lower alcohol, a diol, and water. Preferably, the active agent is a non-steroidal anti-inflammatory drug, such as diclofenac sodium or ibuprofen.
CN101560268A Cs-4 fermentation mycelium polysaccharide and preparation method and applications thereof The invention adopts paecilomyces hepiali Chen (Cs-4) fermentation mycelium as a raw material and uses methods including water extracting, alcohol precipitation, decolorization, ultrafiltration and the like to obtain intracellular polysaccharide of Cs-4 fermentation mycelium of cultured cordyceps sinensis with molecular weight below 500,000. Pharmacological and pharmacodynamic tests show that the polysaccharide provided by the invention has better resistance to glomerular sclerosis and renal interstitial fibrosis and can be used for preparing drugs for resistance to glomerular sclerosis and renal interstitial fibrosis.
EP2768814A1 Novel non-steroidal compounds as androgen receptor modulators This invention relates to novel 4,5-dihydroisoxazoles and 4,5-dihydro[1,2,4]-oxadiazoles of formula (I), to their use as androgenic or antiandrogenic agents or androgen receptor modulators, and to methods of their preparation.
WO2011043435A1 Therapeutic agent for influenza virus infectious diseases Disclosed is a therapeutic agent for influenza virus infectious diseases, which utilizes an active ingredient derived from a natural product and has an excellent effect. Specifically, a β-glucan-containing composition that is obtained from a culture of a microorganism belonging to the genus Aureobasidium is contained as an active ingredient in a therapeutic agent for influenza virus infectious diseases. The therapeutic agent is capable of preventing influenza virus infectious diseases from becoming serious and is capable of promoting the healing of the influenza virus infectious diseases.
US8216599 Administering hydroxytyrosol and oleuropein in a ratio of 1:1-200:1 A method of treating inflammation, an inflammatory condition, or AIDS-associated neurological disorder in a subject in need of such treatment is disclosed. The method includes administering to said subject a pharmaceutically effective amount of substantially purified hydroxytyrosol or a substantially purified mixture of hydroxytyrosol and oleuropein. Also disclosed are compositions for use in practicing the method.
CN103204860A Amaryllidaceae alkaloids compound with neuroprotective effect The invention belongs to the technical field of medicines, relates to Amaryllidaceae alkaloids, and particularly provides Lycoramine compound extracted from lycoris aurea, hybrid lycoris radiata (hybridization of lycoris aurea and lycoris radiata) or other lycoris plants. The compound has protective effect on neural cells, has preventive and curative effect on Alzheimer's disease, and is applicable to preparation of neuroprotective agents and medicines for preventing Alzheimer's disease.
CN101396346A Paclitaxel lipid composite The invention discloses a paclitaxel lipid complex. The paclitaxel lipid complex consists of paclitaxel and lipid material. The weight proportion of the paclitaxel and the lipid material is 1 to 1 - 19, the preferential proportion is 1 to 2 - 10, and the more preferential proportion is 1 to 3 - 6. The lipid material is selected from natural lipid and synthetic lipid or the mixture thereof. The paclitaxel lipid complex can also contain antioxidation stabilizer. The invention also discloses a preparation method of the paclitaxel lipid complex and the application in the preparation of injection submicron emulsion and dry emulsion. The paclitaxel lipid complex has high solubility in oil, and the prepared submicron emulsion has the advantages of high drug loading quantity, high stability, high safety and low irritability.
WO2011118468A1 Wake-time-extending agent Disclosed is a food, beverage or medicinal material which is safe and readily available, does not undergo the deterioration in flavor when combined with another food material or material, is suitably applicable to foods, beverages and medicinal agents, and has a wake-time-extending activity. It is found that an oxidized carotene derivative derived from a terrestrial animal, a terrestrial plant or a microorganism has an activity of shortening a sleep time and extending a wake time.
EP2738173A1 Heterocyclic compounds as inhibitors of the sodium iodide symporter The invention relates to new compounds of formula (I): for their use as medicaments, and in particular as inhibitors of sodium iodide symporter (NIS) and reducers of iodine transport and/or accumulation into NIS-expressing cells. The invention also relates to a pharmaceutical composition comprising at least one compound of formula (I) as active principle. Finally, the present invention relates to specific compounds of formula (I) as such.
WO2009057056A2 Use and device to prevent ventilator acquired pneumonia using nitric oxide A respiratory assist device and use of nitric oxide for the prevention of ventilator acquired pneumonia in a patient is described. The respiratory assist device administers nitric oxide to the oropharyngeal area in order to decontaminate or prevent the contamination of secretions that collect in the oropharyngeal area during intubation of the patient. The respiratory assist device and use of nitric oxide may be adapted for use, for example, as an endotracheal tube or as a tracheotomy tube.
US20090176767 Biphenyl-2-ylcarbamic Acid 1-(2-{5-[2-(4-Hydroxyphenyl)ethylamino]pentylcarbamoyl}ethyl)piperidin-4-yl Ester, used for the treatment of respiratory system disorders such as chronic obstructive pulmonary disease and asthma This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
CN102949501A External washing lotion for treating gynecological inflammation The invention discloses an external washing lotion for treating gynecological inflammation and belongs to the technical field of medicines. The external washing lotion for treating gynecological inflammation is prepared from lightyellow sophora root, common cnidium fruit, phellodendron, dandelion and borneol, has effects of clearing away heat and drying dampness, and killing parasites to relieve itching, and can be mainly used for treating colpitis. The external washing lotion is used clinically for many years and has obvious curative effects.
CN102526019A Use of usnic acid and derivatives of usnic acid for preparation of medicaments for treating skin diseases caused by malassezia The invention belongs to the field of pharmaceuticals, and relates to the new use of an usnic acid and derivatives of the usnic acid, specifically to the use of the usnic acid and the derivatives of the usnic acid for the preparation of medicaments for treating skin diseases caused by malassezia, in particular to the use of the usnic acid and the derivatives of the usnic acid for the preparation of medicaments for treating overmuch scurf, seborrheic dermatitis, atopic dermatitis and psoriasis caused by the malassezia. Inhibition test results show that an average diameter value of an inhibition zone is 20mm and the usnic acid can remarkably inhibit the growth of the malassezia; and a measurement result of a minimal inhibitory concentration (MIC) value of a sodium usnic acid for the inhibition of the malassezia shows that the growth of the malassezia is inhibited along with the rise of a medicinal concentration gradient of the usnic acid and the derivatives of the usnic acid. The usnic acid and the derivatives of the usnic acid disclosed by the invention can be used for preparing the medicaments for treating the skin diseases caused by the malassezia, and can also be used for preparing household chemicals and external preparations for preventing and treating the skin diseases.
CN103351336A Naphthalenecarboxamide derivative as inhibitors of protein kinase and histone deacetylase and preparation method thereof The invention provides a naphthalenecarboxamide derivative as inhibitors of protein kinase and histone deacetylase and a preparation method thereof. The naphthalenecarboxamide derivative is N-(2-methylbenyl)-6-[(7- chloroquinoline-4-oxyl) phenol ether]-2- naphthalenecarboxamide, and the formula of naphthalenecarboxamide derivative is C27H19ClN2O2. The N-(2-methylbenyl)-6-[(7- chloroquinoline-4-oxyl) phenol ether]-2- naphthalenecarboxamide can use as inhibitors of protein kinase and histone deacetylase for curing diseases caused by protein kinase dysregulation. The naphthalenecarboxamide derivative can effectively cure the diseases caused by protein kinase dysregulation, has the advantages of high biological utilization, prominent anti-cancer activity, low toxicity, low preparation cost, high yield, simple and easy-control reaction process, and suitability for industry production.
WO2006044402A1 Furazano `3, 4-b ! pyrazynes and their use as anti-tumor agents The present invention provides novel compounds of the formula (I) and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.
WO2007039821A3 Novel inhibitors of tyrosinase, their method of preparation and their use in human medicine and in cosmetics The present invention relates to novel compounds corresponding to the following general formula (I): to compositions containing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine, or alternatively in cosmetic compositions.
EP1745015A1 Bicyclic aromatic sulfinyl derivatives The present invention provides compounds of formula (I), wherein the constituent members are defined in the claims, pharmaceutical compositions thereof and methods for treating excessive sleepiness associated with narcolepsy, obstructive sleep apnoea or shift work disorder; Parkinson’s disease; Alzheimer’s disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue therewith.
EP2768493A1 Phytocannabinoids for use in the treatment of breast cancer The present invention relates to phytocannabinoids for use in the treatment of a breast cancer. In a first embodiment the invention relates to an oral presentation of tetrahydrocannabinol (THC) for use in the treatment of aggressive breast cancer, characterised by overexpression of the Her2 gene. In a second embodiment the invention relates to the phytocannabinoid cannabidiol (CBD) for use in the treatment of aggressive breast cancer, characterised by overexpression of the Her2 gene. In a third embodiment the invention relates to the combination of the phytocannabinoids tetrahydrocannabinol (THC) and cannabidiol (CBD) for use in the treatment of breast cancer or to treat, prevent or to reduce the risk of a cancer metastasising.
WO2012019021A1 Methods and pharmaceutical compositions for treating adverse or deleterious sequellae of traumatic brain injury This invention provides methods for reducing the extent and progression of traumatic brain injury and its deleterious sequellae specifically cognitive decline, post-traumatic epilepsy, post-traumatic stress disorder, and other adverse consequences depending on the progression of the initial injury, comprising administering to a TBI victim in need thereof a therapeutically-effective amount of an antiglycolytic compound, particularly 2-deoxyglucose (2-DG) or glycolysis-inhibiting analogs thereof. The invention also provides pharmaceutical compositions of 2-DG or glycolysis-inhibiting analogs thereof for use in the methods of the invention.
US7282501 Drugs for treatment of Syndrome X, diabetes, hypoglycemic agents, antilipemic agents, arteriosclerosis and cardiovascular agents The present invention is directed to a compound of formula I, and pharmaceutically acceptable salts, solvates, hydrates or stereoisomer thereof, which are useful in treating Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to Syndrome X as well as cardiovascular diseases.
US7422846 Detecting the activity of orphan G Protein Receptor 86 by incubating a sample comprising GPR86 and adenosine diphosphate (ADP) under binding conditions for both and detecting a second messanger; screening for a modulator The present invention is related to a method of detecting the dysregulation of GPR86 activity.
CN101366707A Application of triacontanol in preparing medicament for treating hyperlipemia, medicament formulation and preparation method thereof The invention relates to application of the prior chemical substance in preparing a pharmaceutical for human use, a prepared oral medicinal preparation and a preparation method thereof. The invention relates to application of triacontanol in preparing a medicine for treating hyperlipemia diseases. The medicinal preparation consists of a medicinal active ingredient, a slow release part and a quick release part. The compositions of the medicinal preparation by weight portion are 90 to 110 of triacontanol, 50 to 70 of ethyl cellulose, 10 to 30 of No. II acrylic resin and 50 to 70 of starch. The preparation method comprises the following steps: firstly, 50 to 70 of the ethyl cellulose and 10 to 30 of the No. II acrylic resin are taken, added with alcohol and dissolved, and then added with half of the weight portion of the triacontanol to prepare soft materials for standby; secondly, 80 to 90 percent of the weight portion of the starch and the other half of the weight portion of the triacontanol are taken and uniformly mixed, the other 10 to 20 percent of the weight portion of the starch is prepared into 10 to 15 percent of starch slurry, and then the mixture and the starch slurry are uniformly mixed to prepare soft materials for standby; and thirdly, particles prepared in the first step and the second step are fully and uniformly mixed, added with adequate talcum powder and uniformly mixed, and a slow release tablet is obtained after tabletting.
US7048943 Carotenoid-loaded liposomes The present invention is based on a novel method for encapsulating in liposomes substantially water immiscible carotenoids. Therefore, there are provided by the present invention formulations comprising liposomes loaded with an amount of at least one water immiscible carotenoid, pharmaceutical compositions comprising such a formulation, and a method for preparing the liposomes loaded with said carotenoid.
WO2006042909A1 Nutrient supplement and use of the same The present invention generally relates to enhancement and recovery of muscle performance in a state of stress induced by physical exercise, disease or trauma. More particularly the invention relates to means for improved muscle performance and for providing more efficient muscle recovery after physical or traumatic stress. The present invention also relates to means for increasing body mass, including muscle mass, and especially lean body mass. Specifically, the invention relates to a nutrient supplement and the use thereof for enhanced recovery and/or performance of the muscles. The invention further relates to a method for improving muscle performance in and muscle recovery from a state of stress induced by physical exercise, disease or trauma.
CA2137668C Benzodiazepines and compositions for treating anxiety and panic disorders, and idiopathic and psychomotor epilepsy The present invention is directed to imidazo[1,5-a][1,4]benzodiazepine-3-carboxamide compounds of formula (I) wherein Ris hydrogen, CH3CH2-, CH2 = CHCH2-, (CH3)2CH-, CH3CH2CH2- or (a), or a pharmaceutically acceptable salt thereof.These compounds and their pharmaceutically acceptable salts possess anti-anxiety and anti-epileptic activity.
CN1879776A Ointment for treating bone fracture Disclosed is a plaster for treating bone fracture which has the active constituents (by weight ratio) of pig bone 25-65g, crab 25-65g, melon seeds 25-65g, processed semen strychni 25-65g, native copper 80-120g, dried body of ground beetle 40-80g, frankincense 25-65g, myrrh 25-65g, cortex acanthopanacis 80-120g, speranskia herb 40-80g, zanthoxylum piperitum 20-40g, drynaria 40-80g, dragon's blood resin 10-30g, sesame oil 1000-1960g and camphor 480-950g.
US20130071408 Methods for Diagnosis and Treatment of Non-Insulin Dependent Diabetes Mellitus Methods and compositions are provided for the treatment and diagnosis of diseases related to hyperglycemic conditions, including diabetes, insulin resistance, and the like. Genetic polymorphisms are shown to be associated with disease susceptibility, and their detection is used in the diagnosis of a predisposition to these conditions. The corresponding proteins are useful as targets for therapeutic intervention.
CN102552910A Application of extracellular matrix protein 1 and regulator thereof in preparing medicament for diagnosing or treating allergic diseases The invention relates to application of extracellular matrix protein 1 (ECM1) and a regulating agent thereof in preparing a medicament for diagnosing or treating allergic diseases. The invention firstly discloses that the ECM1 can regulate migration of Th2 cells, and is closely related to occurrence or development of Th2 cell mediated allergic diseases, so that the ECM1 can be used as a medicinal target to develop a medicament for preventing or treating allergic diseases.
EP2197436A1 Preparation and a component intended to be added to a tobacco product The present invention relates to the use of a preparation comprising a substance that is capable of binding acetaldehyde, and to the use of a filter that is attached to a tobacco product to reduce tobacco and/or alcohol dependence.
US20050197398 mixture of isoleucine, leucine, valine, and alanine, used for treating liver disorders such as hepatitis, cirrhosis or liver cancer Pharmaceutical compositions which contain isoleucine, leucine, valine, and alanine as active ingredients, are useful for treating liver diseases such as hepatitis, liver cirrhosis, liver cancer, and the like via maintenance and improvement of albumin level in blood. In preferred embodiments, the mass ratio of isoleucine:leucine:valine is 1:1.9 to 2.2:1.1 to 1.3; the mass ratio of the total mass of isoleucine, leucine and valine: alanine is 1:0.05 to 10; and a daily dose per person contains isoleucine in an amount of 0.2-30.0 g, leucine in an amount of 0.2-30.0 g, valine in an amount of 0.2-30.0 g, and alanine in an amount of 0.2-50.0 g.
US20080064723 Anti-Hair Graying Agent An anti-hair graying agent containing, as an active ingredient, a substance having a superior anti-hair graying action, for example, aminocyclohexane carboxylic acid, aminocyclohexane carboxylic acid esters such as aminocyclohexane carboxylic acid ethyl ester, aminocyclohexane derivatives such as aminocyclohexanol, and piperidinecarboxylic acid, piperidinecarboxylic acid esters such as piperidinecarboxylic acid ethyl ester, and piperidine derivatives such as hydroxypiperidine is provided.
CN103664922A Novel crystal-form azilsartan and preparation method for same The invention discloses novel crystal-form azilsartan and a preparation method for the same. Characteristic peaks of a PXRD (power X ray diffraction) chart of a polycrystalline form-B azilsartan target are positioned at 2Theta (+/-0.2 degrees, 2Theta) of 7.489, 8.482, 9.384, 13.524, 18.892, 21.147, 23.129 and 25.405, and the melting point is 188 to 190 DEG C. The preparation method comprises the following steps of dissolving azilsartan in methanol, and performing heating reflux until solids are completely dissolved; adding tetrahydrofuran, performing stirring, and performing crystallization at room temperature to obtain the polycrystalline form-B azilsartan target, wherein the using amount of the methanol is about 30 to 70 times the mass of the azilsartan, and the addition of the tetrahydrofuran is about 10 to 30 times the mass of the azilsartan.
US20110064792 Method for Opening Tight Junctions The present invention is directed to a method and use of RNA interference (RNAi) for the transient, reversible and controlled opening of the tight junctions of the blood brain barrier and/or the blood retinal barrier. This method may be used in the treatment of many diseases and disorders which require the opening of the blood brain barrier and/or blood retinal barrier. Such methods generally involve the use of an RNAi-inducing agent, such as siRNA, miRNA, shRNA or an RNAi-inducing vector whose presence within a cell results in production of an siRNA or shRNA, targeting tight junction proteins to open the blood brain barrier and/or blood retinal barrier.
CN103720697A Cyproterone acetate medicinal preparation and preparation method thereof The invention relates to a cyproterone acetate medicinal preparation and a preparation method thereof. The cyproterone acetate medicinal preparation is prepared by taking solutions of cyproterone acetate micro powder particles, a filler, a disintegrating agent, a lubricant, a flow aid and an adhesive as raw materials. The prepared preparation consists of the following components in percentage by mass counted by dry weight: 17-40 percent of the cyproterone acetate micro powder, 40-75 percent of the filter, 1-15 percent of the disintegrating agent, 0-2 percent of the lubricant, 0-2 percent of the flow aid and 0.5-11 percent of the adhesive. As measured by a laser particle size analyzer, the particle sizes of 90 percent by weight cyproterone acetate micro powder particles serving as raw materials are below 5 microns. The dissolution of the cyproterone acetate medicinal preparation can be increased to the maximum extent, so that the bioavailability of the cyproterone acetate medicinal preparation is enhanced; a simple process is adopted, and industrial production is easy to perform.
EP1383563A4 Methods for the treatment of hiv and other viruses A treatment for the persons infected with viruses such as HIV. The method takes advantage of the anesthetic membrane effect brought about by certain gases under pressure. A patient infected with HIV, for example, is placed in a pressurized chamber and exposed to one or more gases under pressure. In this environment, molecules or compounds bind to specific attachment sites on surfaces of host cells and on the virus. These attachment sites are the same sites that are required by the virus to attach to host cells during the virus's replication process. The result is that viruses are prevented from replicating. In the case of HIV, without replication, the virus is also prevented from mutating. This deleterious effect on the virus allows the body's immune system to reconstitute itself in numbers sufficient to cause clinical remission. The present method generally comprises the steps of selecting the gases, pressures and duration to be used inside a pressurized chamber, and exposing the patient to the selected conditions.
US8557855 Methods of using ryanodine antagonists in treating neural injury The present invention provides a method of providing neuroprotection to a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on its nerve cells an effective amount of a ryanodine antagonist, e.g. dantrolene, to inhibit or prevent nerve cell injury or death.
CN101336894A Anticancer composition containing platinum compound and bortezomib An anticancer composition comprising a platinum compound and bortezomib is in form of a sustained-released injection and comprises sustained-released microspheres and a solvent. The sustained-released microspheres comprise an anticancer effective ingredient and a sustained-released adjuvant, and the solvent is a common solvent or a special solvent containing a suspending agent. The suspending agent has a viscosity of 100-3,000cp (20-30 DEG C) and is selected from sodium carboxymethyl cellulose, etc.; the platinum compound is selected from cisplatin, carboplatin and oxaliplatin; and the sustained-released adjuvant is a copolymer or a blend selected from poly(phosphate ester)s such as p(LAEG-EOP) and p(DAPG-EOP), PLA, PLGA, polyphosphate ester-polylactic acid, polifeprosan, poly(erucic acid dimmer-sebacic acid) and poly(fumaric acid-sebacic acid). The anticancer composition can also be made into a sustained-released implant, which can sustain effective drug concentration for more than 40 days by intratumoral or peritumoral injection or placement, and can distinctly reduce the systemic reaction of the drug and selectively enhance the curative effect of non-operative treatments such as chemotherapy and radiotherapy.
WO2013044845A1 Biaryl heterocycle substituted oxazolidinon antibacterial drug The present invention relates to a biaryl heterocycle substituted oxazolidinon antibacterial drug compound as represented by general formula (I), a pharmaceutically acceptable salt, isomer or prodrug thereof, wherein R1, R2, R3, R4, R5, A and B are defined as in the specification; the present invention further relates to a preparation method of the compound, pharmaceutical composition and pharmaceutical formulations containing the compound, and uses thereof in the preparation of drugs for treating and/or preventing infectious diseases and uses thereof in the treatment and/or prevention of infectious diseases.
WO2010026104A1 4-tetrahydropyran-aminopyridine derivatives and their medical use The present invention relates to novel 4-tetrahydropyran-aminopyridine derivatives, to their use in therapy, to pharmaceutical compositions comprising the derivatives, to the use of said derivatives in the manufacture of a medicament, and to therapeutic methods comprising the administration of the derivatives. The present derivatives are useful for treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.
CN102145174A Chondroitin sulfate nano-selenium and preparation method thereof The invention discloses chondroitin sulfate nano-selenium which is granules formed by combining nano-selenium with chondroitin sulfate through sulfuric acid groups, wherein the chondroitin sulfate serves as a carrier, and the mass fraction of selenium is 1-30 percent. In the invention, the chondroitin sulfate nano-selenium is prepared by reducing vitamin C under the mild condition, with the chondroitin sulfate, selenite or selenonic sulfate as a raw material. The method adopted by the invention is an environmentally-friendly synthesis method with simple process and simplesness in operation. The chondroitin sulfate nano-selenium disclosed by the invention is combined with double pharmacological activities of the chondroitin sulfate and the nano-selenium so as to reduce the toxicity of inorganic selenium and improve the bioavailability of the chondroitin sulfate nano-selenium; meanwhile, by combining the biological activity of the chondroitin sulfate, the chondroitin sulfate nano-selenium can be better developed into a novel nano material for preventing and improving osteoarthropathy.
US20060205774 4-(4-(Heterocyclylakoxy) phenyl-1-(heterocyclyl-carbonyl) piperidine derivavites and related compounds as histamine h3 antagonists for the treatment of neurological diseases such as alzheimer's The present invention relates to novel phenyl piperidinyl derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
CA2575777C Compositions and methods for treatment of colitis using methimazole and/or cyclic thione derivatives The present invention relates to the treatment of inflammatory bowel disease (IBD) and related gastrointestinal pathologies. This invention also relates to the treatment of cytokine-mediated diseases, including tumor necrosis factor-.alpha. (TNF.alpha.)-induced diseases and/or chemokine-mediated diseases. This invention also relates to treating an animal having a disease or condition associated with Toll-like receptor (4). Specifically, the present invention relates to the treatment of inflammatory bowel disease (IBD) and related gastrointestinal pathologies that are cytokine-mediated or associated with Toll-like receptor (4). More specifically, this invention is directed to methods for treating or preventing IBD and related gastrointestinal pathologies using methimazole derivatives and tautomeric cyclic thiones. This invention is also directed to pharmaceutical compositions containing methimazole derivatives and tautomeric cyclic thiones, which are useful for the treatment or prophylaxis of IBD and related gastrointestinal pathologies. This invention also relates to pharmaceutical formulations capable of inhibiting tumor necrosis factor-.alpha. (TNF.alpha.)-induced vascular cell adhesion molecule-1 (VCAM-1) expression and the resulting leukocyte-endothelial cell adhesion for the inhibition and prevention of inflammatory bowel syndrome and related gastrointestinal pathologies.
US20080311186 Composition Having Effect on Treatment and Prevention of Dry Eye Syndrome Provided is a composition comprising, as an active ingredient, at least one material selected from the group consisting of uridine and derivatives thereof which promote synthesis of hyaluronic acid in animal and human cell and body, and a pharmaceutical preparation containing the same. The composition and pharmaceutical preparation of the present invention is effective in the treatment and prevention of dry eye syndrome.
CN102793712A Application of chrysin in preparation of medicaments for treating autoimmune and inflammatory diseases The invention discloses application of chrysin in preparation of medicaments for treating autoimmune diseases. Experimental results show that the chrysin can inhibit differentiation of human immune dendritic cells (DC) and maturity of LPS (lipopolysaccharide)-activated human immune DC, can inhibit the antigen uptake capabilities of the immature DC and the antigen presenting capabilities of the mature DC and can inhibit T cell proliferation reactions stimulated by the DC. In particular, the chrysin can reduce the average score, the highest score and the total score of clinical scores of experimental autoimmune encephalomyelitis of mice and can relieve myelitis cell infiltration and demyelination in spinal cords. Thus, the medicament inhibiting immune systems is expected to become the medicament for treating such autoimmune inflammatory diseases as multiple sclerosis, neuromyelitis optica and acute disseminated encephalomyelitis clinically.
WO2005058875A1 Piperazine triazine compounds, preparation thereof and pharmaceutical compositions The invention provides piperazine triazine compounds of Formula (I) and They’re pharmaceutically acceptable salts: Formula (I) wherein: R1 is hydrogen, C1-C4alkyl, aryl, substituted aryl, aralkyl, C1-C4alkanoyl, aroyl or C3-C7cycloalkyl; R2 and R3 are respectively aryl, substituted aryl, aralkyl, C1-C4alkaryl or C3-C7cycloalkyl; X is NR7,O,S;R4 and R6 are respectively hydroxyl or C1-C6alkyl; R5 is hydroxyl, C1-C6alkyl,-C(O)R8,-(CH2)mR8,-CH2CH=CHR8,-C(O)OR8,-C(O)OR8 or S(O)2R8, m is 0,1,2 or 3; R7 is hydrogen, hydroxyl or C1-C6alkyl; R8 is hydrogen, hydroxyl, aryl, heteroaryl, heterocyclic radical or C2-C6alkenyl. It is approved that the piperazine triazine compounds of the present invention are epoxy synthase (COX-1 and COX-2) inhibitors with fine curative effect and prevention to clinic inflammation through computer virtuality screening, epoxy synthase(COX-1 and COX-2) combination experiment and pharmacological test. Preparation and pharmaceutical compositions of the compounds are also provided.
US7053070 Antiproliferative agents; anticarcinogenic agents; viricides Disclosed are compounds of the formula wherein R2, R5, R6, R7, and R8 are as defined herein. These compounds and their pharmaceutical compositions are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cdks and growth factor-mediated kinases.
WO2009054150A1 Tetrapyrrole derivative, and use thereof for medical purposes [PROBLEMS] To provide an agent for preventing a diabetic neuropathy, which does not induce any hypotensive effect or hyperkalemia. [MEANS FOR SOLVING PROBLEMS] Disclosed is an agent for preventing a diabetic neuropathy, which comprises a tetrapyrrole derivative represented by the general formula (I) or a pharmaceutically acceptable salt or ester thereof as an active ingredient.
CN102083446A Biological markers and response to treatment for pain, inflammation, neuronal or vascular injury and methods of use The present invention provides methods and kits for treatment of pain, inflammation, neuronal or vascular injury and the use of biomarkers for the assessment of the biological activity or disease state. In one embodiment, the kit comprises a biomembrane sealing agent, such as PEG, a bioactive agent, such as a magnesium compound, and an assay for measuring a biomarker. The biomarker is measured pre-, mid- and post-treatment, and results of the measurements are compared to evaluate the treatment, treatment regimen and outcomes.
CN103520702A Cow udder cleaning agent used for preventing bovine mastitis The invention discloses a cow udder cleaning agent used for preventing bovine mastitis and relates to a cleaning agent for cleaning cow udders. The invention aims at solving the problem that an existing cow udder cleaning agent is poor in effect of inhibiting and killing bovine mastitis-causing bacteria and easily causes iodine content in milk to exceed standards. The cow udder cleaning agent consists of nisin, epsilon-polylysine (epsilon-PL), EDTA (Ethylene Diamine Tetraacetic Acid) disodium, glycerin, citric acid, polyvinyl pyrrolidone and the balance of pure water. The cow udder cleaning agent used for preventing bovine mastitis, disclosed by the invention, has a good killing effect for pathogenic bacteria that cause bovine mastitis, and has a sterilizing rate of 100% for escherichia coli, staphylococcus aureus and streptococcus agalactiae; meanwhile, the cow udder cleaning agent does not contain iodine and solves a problem that the iodine content in milk easily exceeds the standards. The cleaning agent disclosed by the invention is mainly applied to cleaning and sterilizing the cow udders before and after milking the cow.
US20090062284 Thio-Substituted Biarylmethanesulfinyl Derivatives The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
US20080027029 Cold menthol receptor-1 antagonists The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
CN102552227A Application of shikonin derivatives to preparation of pyruvate kinase inhibitors The invention mainly relates to application of five shikonin derivatives to preparation of pyruvate kinase inhibitors. The shikonin derivatives are one of deoxyshikonin, isobutyryl shikonin, beta,beta-dimethylacrylshikonin, Isovalerylshikonin and [(2-methyl-n-butyl)shikonin. A currently reported M2 pyruvate kinase (PKM2) inhibitor is Compound 3. According to the invention, natural shikonin derivatives have higher inhibiting effects on the PKM2 compared with the Compound 3. The natural shikonin derivatives serving as pyruvate kinase inhibitors have important application value. The invention has the advantages that: the five new pyruvate kinase inhibitors, namely natural shikonin derivatives, provide bases for screening of new medicines and have important application prospects.
US20080312222 4-Benzyledene-Piperidin Derivatives The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.
US20110076252 Compound and method for treatment of gastroesophageal reflux The invention relates to the use of a L-theanine for the treatment of gastroesophageal reflux disease (e.g., heart-burn) in a human or animal, including useful methods and compositions.
CN101607886A Novel wool gonane compound as well as preparation method and anticancer purpose thereof The invention provides a novel wool gonane compound as well as a preparation method and an anticancer purpose thereof. The wool gonane compound is shown as the right general formula (I); and an anticancer activity test indicates that the novel wool gonane compound has obvious anticancer activity, wherein R1 and R2 in the formula are respectively and independently selected from hydrogen and alkyl with 1-6 of carbon number.
EP1756084B1 Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto The present invention relates to certain substituted aryl and heteroaryl derivative of Formula (I) that are modulators of metabolism, especially of the activity of a GPCR, referred to herein as RUP3. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.
EP2688564A2 Calcium supplement An oral dosage form for administration to an animal comprising a biologically utilizable form of calcium and a extended release system that maintains the calcium level in the animal's bloodstream at a substantially beneficial level for a defined period of time.
WO2008151927A2 6-n-substituted benz imidazole derivatives as acid pump antagonists The invention provides compounds of the formula (0), in which the substituents and symbols are as defined in the description. The compounds inhibit the secretion of gastric acid.
WO2009147441A2 Novel treatments The present invention relates to the treatment of the premonitory symptoms of migraine, to the treatment of aura associated with or without migraine, epilepsy, non-epileptic seizures, stroke or other cardiovascular disorders, to the pre-emptive treatment of aura, migraine, epilepsy, stroke or other cardiovascular disorders, to the treatment of migraine recurrence or aura recurrence,and to tonabersat, co-crystals thereof, and compositions comprising tonabersat for use in said treatments.
US20130005708 Histamine antagonist treatment of inflammatory skin disorders Presented herein inter alia are compositions, methods, and kits for treating an inflammatory skin disorder using a histamine antagonist. In certain embodiments, the compositions, methods, and kits are for treating urticaria and its symptoms. In certain embodiments, the composition, methods, and kits include a topical pharmaceutical preparation with an effective amount of alcaftadine as an active agent.
EP1546103B1 Piperazine and piperidine derivatives for treatment of neurological diseases The present invention relates to piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage of for stimulating nerve growth.
EP1689385B1 Neuroactive substance and uses of one such substance The invention relates to a neuroactive substance which is characterised in that it has formula (O), wherein R1, R2, R3 and R4 are identical or different and are methyl or ethyl radicals. Preferably, the neuroactive substance comprises 6S-acetyl-4R,5R-dimethyl-1R(10S)-epoxy-2R-hydroxy-7R-acetoxydecahydro naphthalene which can be isolated from Rhytisma fulvum cnidaria. The inventive neuroactive substance can be used as a pharmacological reagent in research work and is also suitable for use in the fields of industry (insecticides) and health, such as for the treatment of Parkinson's disease.
CN102727507A Gastrodia elata parishin extract freeze-dried powder injection and preparing method therefor The invention discloses a gastrodia elata parishin extract freeze-dried powder injection. The freeze-dried powder injection contains a gastrodia elata parishin extract, selectively contains a freeze-drying excipient. Total content of parishin derivatives in the gastrodia elata parishin extract accounts for more than 50%. Weight percentage of the parishin derivatives in the freeze-dried powder injection accounts for 0.1% to 100%, preferably accounts for 50% to 100%. Also disclosed is a preparation method for the freeze-dried powder injection. The freeze-dried powder injection in invention is advantaged in good stability, easiness in storage and transport, precise curative effect and the like.
CN103735571A Application of hydrogen sulfide and donor thereof in improving sperm quality and function The invention discloses an application of hydrogen sulfide and donor thereof in improving the sperm quality and function, and relates to the field of reproduction. The hydrogen sulfide can be directly added into semen in vitro, and the activity of the sperms of clinical asthenospermia patients can be remarkably improved within short time. The hydrogen sulfide also can resist oxidative stress for the sperms cultured in vitro so as to reduce the stress injury of the sperms caused by manual operation and in-vitro culture and maintain the activity level of the sperms. The hydrogen sulfide also can be used for improving the dyszoospermia caused by infection, protecting the spermatogenic structure of testis, maintaining the completion of blood-testis barrier and the synthesis of androgen, reducing the inflammatory level in the testis tissue and the oxidative stress of spermatogenic cells, and reducing the apoptosis of spermatogenic cells caused by infection so as to maintain a normal spermatogenic process, keep the sperm quality and maintain normal fertility of male. The invention opens up a new application field of hydrogen sulfide and provides a significant reference to solving the human dysgenesis and improving the assisted reproductive technology.
CN103446116A Applications of Sarcaboside B in medicament against herpes virus The invention discloses applications of Sarcaboside B in preparing a medicament against herpes virus. Experiments prove that the Sarcaboside B plays a remarkable role in inhibiting Herpes simplex virus HSV-1 and Herpes simplex virus HSV-2, thus indicating that the Sarcaboside B has potential application values in the field of treating herpes virus-infected diseases. The applications disclosed by the invention provide an experimental basis for the Sarcaboside B in clinically treating herpes virus-infected diseases, and offer certain guiding significance for developing medicaments against HSV-1 and HSV-2, thus having an important reference value.
US20110076332 Dextran-chitosan based in-situ gelling hydrogels for biomedical applications A biodegradable hydrogel comprises a water-soluble dextran having aldehyde groups cross-linked with a water-soluble chitosan. Various chemical agents may be encapsulated in the hydrogel or bonded thereto for controlled release. The hydrogel may be applied as a coating to reduce the likelihood of bacterial attachment and biofilm growth; used in tissue engineering applications to prevent tissue ingrowth; or used as a matrix in which cells may proliferate. The components of the hydrogel can be applied sequentially as a spray or by immersion and will gel spontaneously at environmental or physiological temperatures.
US20060004065 5,5,7,9,13-%-Pentamethyl-16-[1-methyl-2-(2-methyl)-1,3-thiazol-4-yl)-ethenyl]-6,6-dioxo-1-ox-a-6 lambda 6-thia-cyclohexadeca-10,13-dien-2-one; epothilones and derivatives; improved properties; anticarcinogenic, -tumor agents The present invention relates to new Macro-cycles of Formula (I), and their use for the treatment of cancer.
EP1478398B1 New medicinal compositions on the basis of anticholinergic agents and egfr kinase inhibitors The invention relates to novel medicinal compositions on the basis of anticholinergic agents and EGFR kinase inhibitors, methods for the production thereof, and the use thereof for treating respiratory diseases.
CN102391191A Piperazine di-thiocarboxylic acid ester derivative of 2,4-di-aminoquinazoline, as well as preparation method and anti-tumor application of the derivative The invention discloses a piperazine di-thiocarboxylic acid ester derivative of 2,4-di-aminoquinazoline, as shown in a general formula (I), wherein R refers to C1-6 straight-chain or branched-chain alkyl group or substituted C1-6 straight-chain or branched-chain alkyl group, or C3-6 naphthenic group, or aryl group or substituted aryl group, or heteroaryl group. In addition, the invention discloses a preparation method and a pharmaceutical composite of the compound, namely piperazine di-thiocarboxylic acid ester derivative. The compound shown in the general formula (I) plays a role in restraining cells of human lung cancer (A-549), human breast cancer (MFC-7) , human colon cancer (HT29 and HCT-116) and human cervical cancer (HeLa) and can serve as an anti-tumor medicament.
WO2009114139A3 Methods, compositions, and kits for treating pain and pruritis The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.
US20050153978 Medicaments A method of treating an Msk-1 and/or ROCK(1 and 2) mediated disease or condition in a mammal comprising administration of an effective amount of a compounds of the formula (I) and physiologically acceptable salts thereof wherein, R1 is a 5, or 6 membered heterocyclic group selected from group a, b, c or d wherein X1 is a group selected from N or CR7 and X2 is a group selected from O, S or NR8; X3 and X4 which may be the same or different is a group selected from N or CR7; X5 is a group selected from O, S or NR8 and X6 is N or CR7; X7, X8 and X9 may be the same or different and selected from a group N or CR7, pharmaceutical compositions, novel compounds and processes for their preparation.
US20110224183 16, 17-carbocyclic condensed steroid compounds having slective estrogenic activity The invention discloses a steroid compound having the formula (1): wherein dotted bonds represent optional double bonds; R6 is H, ═CH2, or —CH3, or —CH2—CH3; R7 is H, C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, Cl1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being α and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.
US7268222 For use in therapeutic, diagnostic, and pharmacogenomic applications Novel human ATP binding cassette transporter polynucleotide and polypeptide sequences are disclosed that can be used in therapeutic, diagnostic, and pharmacogenomic applications.
US7001894 Blood flow improvers and thrombosis preventives or remedies Glucosamine salts and derivatives are effective for the improvement of blood flow, and hence, for the prevention and/or treatment of diseases caused by blood flow disturbances, such as thrombosis. Use of glucosamine salts or glucosamine derivatives as active ingredients can provide blood flow improvers, thrombosis preventives or remedies, and dietetic drinks or foods for the improvement of blood flow or for the prevention and/or treatment of thrombosis. Administration of glucosamine salts or glucosamine derivatives can improve blood flow and can prevent and/or treat thrombosis.
US20080194494 4-Biarylyl-1-Phenylazetidin-2-One Glucuronide Derivatives for Hypercholesterolemia The invention relates to a chemical genus of 4-biarylyl-1-phenylazetidin-2-ones useful for the treatment of hypercholesterolemia and other disorders, having general formula: Pharmaceutical compositions and methods for treating cholesterol- and lipid-associated diseases are also disclosed.
US20110135755 Combination therapies for treating neoplastic disease A method for treating neoplastic disease in a patient is described, which comprises administering to the patient: an antineoplastic platinum (II) complex; a physiologically acceptable source of assimilable copper; a physiologically acceptable source of assimilable manganese; a source of salicylic acid or a physiologically acceptable derivative thereof; and vitamin C.
US7071165 LHRH antagonist peptides Novel LHRH antagonist peptides, pharmaceutical compositions thereof, and methods of use thereof, are disclosed. The LHRH antagonist comprise a peptide compound, wherein a residue of the peptide compound corresponding to the amino acid at position 6 of natural mammalian LHRH comprises a hydrophilic N-acyl moiety, a dipolar moiety, a sulfonium moiety, a receptor-modifying moiety or a small polar moiety.
US20100273844 Pharmaceutical compositions for treating or preventing migaines The present invention provides a method for treating or preventing one or more types of migraines by administering a monoamine oxidase inhibitor, preferably isocarboxazid, in a rapid-release formulation. The present invention also provides a pharmaceutical composition suitable for treating or preventing migraines and having at least one monoamine oxidase inhibitor.
EP1115849B1 Genes of the 1-desoxy-d-xylulose biosynthetic pathway The invention relates to the 1-desoxy- D-xylulose- 5-phosphate reductoisomerase gene, the 1-desoxy- D-xylulose- 5-phosphate- synthase gene and the gcpE gene of the 1-desoxy- D-xylulose biosynthetic pathway and to their use for transforming vectors, host organisms and plants and for determining substances that inhibit this biosynthetic pathway.
CN102961385A Pharmaceutical formulation for treating psoriasis The invention relates to a pharmaceutical formulation for treating psoriasis. The pharmaceutical formulation is prepared through mixing alcohol, salicylic acid, benzoic acid, penicillin and rivanol. The pharmaceutical formulation has a short treatment course of generally 3-5 days; the pharmaceutical formulation is an externally applied medicament, is applied to affected parts for one to two treatment courses, the curative ratio reaches above 90%, and 85% of patients are radically treated; and the pharmaceutical formulation is safe to use and does not have toxic and side effects.
CA2376916C Anaesthetic formulation comprising an nmda-antagonist and an alpha-2 adrenergic agonist A pharmaceutical composition is described. The composition comprises a formulation. The formulation comprises an NMDA antagonist and an alpha 2 adrenergic agonist. In a preferred aspect, there is provided an improved anaesthetic comprising an NMDA antagonist and an alpha-2 adrenergic agonist.
EP1905442A1 Utilization of anti-neuropathic pain effect of d-allose and d-psicose PROBLEMS To control neuropathic pain produced by various mechanisms. [MEANS FOR SOLVING PROBLEMS] Disclosed is a composition for elimination, relief or reduction of neuropathic pain comprising, as an active ingredient, at least one substance selected from the group consisting of D-allose, a derivative ofD-allose, D-psicose and a derivative of D-psicose preferably in an amount of 0.01 to 90% by weight. The composition may comprise a mixture of D-allose and/or a derivative thereof and D-psicose and/or a derivative thereof at a ratio of 1:1 to 10:1. The neuropathic pain may be one induced by a disease selected from the group consisting of trigeminal neuralgia, postoperative pain, periodontitis, gingivitis, gingivostomatitis, oral ulcer, herpes zoster, postherpetic neuralgia, diabetic neuritis, causalgia, phantom limb pain and malignant tumor. Also disclosed is use of the composition for elimination, relief or reduction of neuropathic pain by administering the composition to a patient with neuropathic pain in such an amount that 0.01 to 100 g of the at least one substance can be taken by the patient per day.
CN103463542A Application of edible vinegar as liquor for removing scars and changing skin, liquor for removing scars and changing skin and preparation method of liquor The invention discloses application of edible vinegar as a liquor for removing scars and changing skin, the liquor for removing scars and changing skin and the preparation method of the liquor. The liquor for removing scars and changing skin is prepared from the following raw materials by weight percent: 8-12% of salicylic acid, 18-22% of rhizoma galangae and 68-72% of edible vinegar. The preparation method of the liquor comprises the following steps: A, smashing, namely choosing out the rhizoma galangae according to the ratio and smashing into fine particles; B, soaking, namely weighing the salicylic acid according to the ratio, and then putting into the edible vinegar weighed according to the ratio to soak for 28-32 days together with the rhizoma galangae in the step A, and then filtering out residue to prepare the liquor, concentrating the liquor to 88-92%, so as to obtain the product liquor. According to the liquor, just a simple formula and available raw materials are selected. Compared with the prior art, the preparation method is easier to implement, low in cost, and easy to be accepted by a sufferer. The liquor has a function of removing the scars, and is fast to take effect, high in recovery rate, free of toxic and side effects and good in safety.
CN1699401B Novel anti-cancer active compound and its extraction process The invention relates to an anticancer reactive compound extracted from Asterias rollestoni Bell, an ocean creature, wherein the preparation comprises freezing and disintegrating the collected samples, dipping three times with 10 times of ethanol, merging the raffinate, decompression reclaiming to drying, suspending the residues with water, abstracting with petroleum ether, acetic acid ethyl esterand normal butyl alcohol, merging with acetic ester extraction portion, decompression reclaiming and passing through multi-time silica gel column color spectrum and gel column chromatography, finallyobtaining the monomer compound through high performance liquid phase purification. The compound can be used in preparing anti-cancer medicaments.
CN101367787A Mango aglycone, preparation purification process and uses thereof The present invention belongs to the technical field of biological pharmacy, and in particular relates to a preparation and purification method of tetra-hydroxyl xanthone mango aglycone (norathyriol), and an application thereof in hypoglycemic medicine. Based on biological experiments, mango glycoside is used as raw material; under the condition with phenol and hydroiodic acid, carbon-carbon bonds are broken to produce the crude product of mango aglycone; the crude product is separated and purified through silica gel column chromatography so that the mango aglycone is separated; the yield rate reaches 12 percent, the purity is higher than 95 percent, and the reproduction performance is good; the IGTT of C57BL/6 normal mice is effectively improved with the norathyriol; and simultaneously the quantity of insulin secretion induced by glucose in vivo for the C57BL/6 normal mice can be improved with the norathyriol. Therefore, the mango aglycone can be applied for preparation of hypoglycemic medicine.
EP1455799B1 Pharmaceutical combinations of adenosine a-2a and beta-2-adrenergic receptor agonists The present invention relates to a combination comprising (a) an adenosine A2a receptor agonist as defined herein and (b) an adrenergic β2 receptor agonist, for simultaneous, sequential or separate administration by the inhaled route in the treatment of an obstructive airways or other inflammatory disease.
WO2007104783A3 1,4 -di substituted 3-cyano-pyridone derivatives and their use as positive mglur2-recept0r modulators The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - sub- type 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical composit ions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
WO2010124141A1 Methods of treating a pulmonary bacterial infection using fluoro-quinolones Disclosed herein are methods of treating a pulmonary bacterial infection comprising bacteria growing under anaerobic conditions using a fluoroquinolone antibiotic. The fluoroquinolone antibiotic may, for example, be levofloxacin or ofloxacin. Also disclosed are methods of inhibiting bacteria growing under anaerobic conditions by exposing the bacteria to an amount of fluoroquinolone antibiotic effective to inhibit growth of said bacteria.
US20120142646 Novel Compounds 621 The present invention provides compounds of formula (I) wherein k, Ar, R2, R3, R4, R5, R4′, R5′, R6, R7, A, D, m and E are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
US20090053286 Products and methods for maintaining or increasing ceramide levels in skin Disclosed are methods and products such as wet wipes and absorbents capable of providing a skin health benefit when utilized in the intended fashion. More specifically, the products described herein comprise an agent, such as a botanical extract, which is capable of increasing the activity of sphingomyelinase according to a Sphingomyelinase Activity Screening Test and/or decreasing the activity of ceramidase according to a Ceramidase Activity Screening Test. By increasing the activity of sphingomyelinase and/or decreasing the activity of ceramidase, the agents in combination with the products described herein are able to maintain or increase the level of ceramides in the skin leading to improved skin health.
CN101569701B Improved method for preparing 3.5g refined menthocamphorate The invention relates to an improved method for preparing 3.5g refined menthocamphorate. The formulation adopted by the method comprises camphor, clove oil, camphor oil, dragon blood solution, strong ammonia solution and paraffin. The method is characterized in that: by calculating total weight of 1,000g, the formula also comprises 10 to 140g of menthol, 40 to 120g of dementholised peppermint oil, 20 to 35g of ozokerite and 180 to 477g of yellow vaseline. The invention also provides a preparation process adopted by the method, which mainly comprises steps of mixing and stirring mixed oil, substrate and the strong ammonia solution prepared, and cooling, filling and packaging the mixture. For the 3.5g refined menthocamphorate prepared by the process according to the formulation, detection indexes all reach the quality standard, and the melting point reaches the top-grade product standard (the melting point is between 45 and 60DEG C, and the volatile oil quantity is more than or equal to 1.7ml/5g). The method and the process can reduce product cost, ensure product quality, and meet the quality standard.
WO2010132047A8 Guanosine/gmp gels and uses thereof The invention relates in some aspects to guanosine/GMP gel compositions for delivering antibodies, nucleic acids, and particles. In other aspects the invention relates to guanosine/GMP gel compositions and methods of use thereof for controlled-release of antibody, nucleic acid, and micro- and nano-particles.
CN103193604A Asarin compound and freeze-dried powder injection thereof The invention discloses an asarin compound with a brand new activity. Both the asarin compound and a preparation thereof are remarkably superior to conventional asarin compounds in a stability test and the like. As the stability of the preparation can be remarkably improved by the asarin compound, the medication safety of patients can be guaranteed. Besides, the invention further discloses a preparation method of the asarin compound and a freeze-dried powder injection containing the asarin compound.
EP1869000A1 Cyclopentapyridine and tetrahydroquinoline derivatives 6,7-Dihydro-5H-cyclopenta[b]pyridine and 5,6,7,8-tetrahydroquinoline compounds of Formula (I), including salts, hydrates and solvates thereof, that act as 5-HT2 receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2C receptors are described herein.
CA2811318A1 Concentration and mental performance amplifying formulation A concentration and mental performance amplifying formulation comprising rhodiola rosea, geranium oil, vinpocetine, phosphatidylcholine, caffeine and Salix alba (White Willow Bark).
WO2014056280A1 Microencapsulated amino acid composition and preparation method thereof Disclosed are a microencapsulated amino acid composition and the preparation method thereof.The microencapsulated amino acid composition is obtained as follows: a raw material mixture containing the amino acid is added into water or ethanol solution, then prepared by granulating and drying; wherein the raw material mixture comprises the following components: a. single amino acid or multiple amino acids; b. the auxiliary material containing a coating agent and wetting agent.
WO2014009966A3 An improved process for the preparation of dabigatran etexilate mesylate and its intermediates thereof An improved process for the preparation of Dabigatran Etexilate Mesylate and the processes for the preparation of Dabigatran single prodrug and Dabigatran Etexilate are described in this invention
US20080299188 Controlled release dosage forms combining immediate release and sustainted release of low-solubility drug A controlled release dosage form comprises an immediate release portion and an enteric coated sustained release core.
US8586604 Inhibitors of the microsomal prostaglandin E2 synthase-1 This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7 have meanings given in the description.
EP2768797A1 Novel modified curcumins and their uses This invention provides a compound having the structure (I) wherein α, β, A, B, and R1-R4 are defined herein. This invention also provides pharmaceutical compositions comprising the above compounds, a method of accelerating the healing of a wound, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NFK-B activation in a population of cells.
WO2006000339A3 Calcium trifluoroacetate for preparing antiangiogenetic medicaments Calcium trifluoroacetate, known to have cytotoxic activity, is endowed With of antiangiogenetic activity and can be used for the therapy of atherosclerotic plaque, rheumatoid arthritis, psoriasis, diabetic retinopathy, rosacea, cheloids, metastasis.
WO2004082669A3 Antiflatulents in combibation with histamine h1-receptor antagonist for treating gastrointestinal disoders Compositions and methods for providing relief from pain and/or discomfort associated with gastrointestinal disorders, including, for example, bloating, crying, gas, cramping, regurgitation, diarrhea and gastrointestinal pain, associated with colic comprising, at least one antiflatulent, at least one histamine H1-receptor antagonist, and optionally,one or more prebiotic and/or one or more probiotic.
US7655676 Selective activity against propionibacterium acne; minimum inhibitory concentration (MIC) against Propionibacterium acnes strains both sensitive and resistant to erythromycin and clindamycin and against a series Staphylococcus strains Use of the compound of formula (I) and the pharmaceutically acceptable addition salts thereof for the manufacture of a medicament for topical treatment or 5 prevention of acne formula (I) wherein: R represents methoxymethyl, R1 represents methyl, Rz represents methyl, Y represents the group formula (II) The compound of formula (I) and the pharmaceutically acid addition salts thereof show selective activity against propionibacterium acne and are suitable for use in a method of treatment or prevention of acne.
CA2387247C Use of neutralizing agents to growth factors for reducing wound scarring A composition for use in the treatment of wounds to inhibit scar tissue formation during healing is disclosed, comprising an effective activity-inhibiting amount of a growth factor neutralising agent or agents specific against only fibrotic growth factors together with a pharmaceutically acceptable carrier. The method of preparation of said composition and method of administering the composition to a host suffering from tissue wounding is also disclosed.
US20100120893 Compositions and Methods for Inhibiting Expression of Transthyretin The invention relates to a double-stranded ribonucleic acid (dsRNA) targeting a transthyretin (TTR) gene, and methods of using the dsRNA to inhibit expression of TTR.
EP2114397A2 Novel conjugates of polyunsaturated fatty acids with amines and therapeutic uses thereof The present application discloses conjugates comprising an aminic moiety covalently linked to a hydrophobic moiety, through an amidic bond, which are selective inhibitors of COX-2 enzyme and can be beneficially used in the treatment of various inflammatory disease or disorder and cancer.
CN1872169A Compound gel of rhinitis, and preparation method A medicine in the form of gel for treating rhinitis is prepared from ephedrine hydrochloride, benadryl hydrochloride, and the concentrated liquid extracts of green chiretta and small centripeda herb through dissolving in water, filtering, stirring, adding mint oil and eucalyptus oil, stirring, adding triethanolamine or sodium hydroxide or ammonia water to regulate pH value, adding humectant, adding water and stirring.
WO2014125052A1 Pharmaceutical composition for oral administration comprising fexofenadine and process for preparing thereof The present invention relates to pharmaceutical compositions for oral administration, said compositions comprising high(methyl)pectin, glycerol,water and fexofenadine,or a pharmaceutically acceptable salt thereof. The invention also relates to the uses of these compositions as a medicament and to the process for preparing said compositions.
US20100291084 Use of il-23 antagonists for treatment of infection Methods and compositions comprising antagonists of IL-23 are provided for the treatment of infections, such as chronic bacterial, viral and fungal infections.
US20120093759 Medical Devices, Wound Dressings, and Methods for Dressing Wounds Medical devices, wound dressings, and methods of dressing wounds are described. Devices and methods using silicone and pharmaceutically active agents are described. Devices including covers and bases are described.
US20120095042 Organic Compounds Having Cooling Properties Provided are compounds of formula (I) wherein m is 0, 1 or 2; RI is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R2 is selected from hydrogen, methyl and ethyl; I) R3 is hydrogen, methyl, or ethyl; and R4 and R5 are independently selected from ethyl and isopropyl; and R3, R4 and R5 together have at least 6 carbon atoms: or II) any two or all of R3, R4 and R5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.
US20050070558 For example, [4-(2,4-Dioxo-1,3-dipropyl-2,3,4,5-tetrahydro-1H-pyrrolo[3,2-d]pyrimidin-6-yl)phenoxy]acetic acid; useful in preventing mast cell degranulation and therefore useful in treatment of diseases induced by activation of A2b receptor and mast cell activation such as asthma, allergic reactions 6-phenylpyrrolopyrimidinedione derivatives of the formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are organic residues, L1 is a spacer group and R6 is C(O) NR10R11, —S(O)2NR10R11, ? —ON═CR12R13, or a heterocyclyl, aryl? or heteroaryl group, where R10, R11, R12 and R13 are organic residues, have therapeutic potential as A2 adenosine receptor inhibitors.
US20130004453 Nylon-3 co-polymers and synthetic lung surfactant compositions containing same Non-natural oligomers have recently shown promise as functional analogues of lung surfactant proteins Band C (SP-B and SP-C), two helical and amphiphilic proteins that are clitical for normal respiration. The generation of non-natural mimics of SP-B and SP-C has previously been restlicted to step-by-step, sequence-specific synthesis, which results in discrete oligomers that are intended to manifest specific structural attributes. Presented herein an alternative approach to SP-R mimicry that is based on sequence-random copolymers containing cationic and lipophilic subunits. These materials, members of the nylon-3 family, arc prepared by ling-opening polymelization of 13-lactams. The best of the nylon-3 polymers display promising in vitro surfactant activities in a mixed lipid film. Pulsating bubble surfactometry data indicate that films containing the most surface-active polymers attain adsorptive and dynamic-cycling properties that surpass those of discrete peptides intended to mimic SP-B.
CN103006846A Application of Qingkailing to preparation of medicament against multiple resistant bacteria The invention relates to application of Qingkailing to preparation of a medicament against multiple resistant bacteria. Qingkailing has an inhibiting effect on multiple resistant bacteria containing NDM-1 drug-resistant genes, acinetobactercalcoaceticus, acinetobacterbaumannii and escherichiacoli containing NDM-1 drug-resistant genes. In addition, combined with twenty clinical common antibiotics, Qingkailing injection also has an inhibiting effect on acinetobacter calcoaceticus, escherichia coli containing NDM-1 drug-resistant genes and stenotrophomonasmaltophilia. Therefore, Qingkailing can be used separately or combined with antibiotics to treat and/or prevent diseases caused by bacteria containing NDM-1 drug-resistant genes.
US20120283301 S-triazolyl alpha-mercapto acetanilides as inhibitors of hiv reverse transcriptase A series of S-triazolyl α-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
US20080286351 Pegylated Cardiolipin Analogs, Methods of Synthesis, and Uses Thereof The invention provides synthetic methods for PEGylated cardiolipins with varying linkers. The methods can be employed to prepare PEGylated cardiolipin with different fatty acid and/or alkyl chain length with or without unsaturation. The PEGylated cardiolipin, prepared by the present methods, can be incorporated into liposomes that can also include active agents such as hydrophilic or hydrophobic drugs for the treatment of human and animal diseases. In addition, the PEGylated cardiolipin can be incorporated into liposomes that include compounds for therapeutic and diagnostic imaging. The use of such liposomes with PEGylated cardiolipin prolongs the period of liposomal circulation without disrupting the lipid bilayer.
CN101302204A Quinazolone compound, composition and application including the same Quinazolinones of formulae (1c and 1d) are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.
US20090012085 Dosage forms and methods of treatment using a tyrosine kinase inhibitor This invention provides dosage forms of a compound of formula 1, 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, or pharmaceutically acceptable salts or solvates thereof. The invention further provides methods of treating abnormal cell growth in a patient, such as cancers, by administering the dosage forms to the patient. The invention further provides methods of treating an angiogenesis- or VEGF-related ophthalmic disorder in a patient, by administering the dosage form to the patient.
CN103242400A 5-substituted pyrimidine nucleoside-thiazolidinone hybrid with anti-HIV activity and preparation method thereof The invention discloses a 5-substituted pyrimidine nucleoside-thiazolidinone hybrid with anti-HIV activity and a preparation method thereof. In a structural formula of a compound A, R1 represents one of (2R, 4S, 5S)-4-azido-2, 3, 4, 5-tetrahydro-5-(acetyloxy)methyl furan-2- group, (2R, 4S, 5S)-4-azido-2, 3, 4, 5-tetrahydro-5-hydroxymethyl furan-2- group, (2R, 5S)-2, 5-dihydro-5- (acetyloxy)methyl furan-2- group, (2R, 5S)- 2, 5-dihydro-5- hydroxymethyl furan-2- group; and R2 represents one of phenyl, substituted phenyl, pyridyl, substituted pyridyl, alkyl, naphthenic, propargyl, benzyl, etc. The 5-substituted pyrimidine nucleoside-thiazolidinone hybrid with anti-HIV activity, contains at least one compound A, or an additive salt formed by a pharmaceutically-acceptable acid or alkali, individually or combining one or more pharmaceutically-acceptable, inert and nontoxic excipients or carriers, forms a pharmaceutical composition, and the pharmaceutical composition is used for preparing an anti-AIDS medicament.
US20060165652 Immunotherapy with in vitro-selected antigen-specific lymphocytes after non-myeloablative lymphodepleting chemotherapy A method of promoting the regression of a cancer in a mammal comprising: (i) administering to the mammal nonmyeloablative lymphodepleting chemotherapy, and (ii) subsequently administering: (a) autologous T-cells, which have been previously isolated, selected for highly avid recognition of an antigen of the cancer, the regression of which is to be promoted, and rapidly expanded in vitro only once, and, either concomitantly with the autologous T-cells or subsequently to the autologous T-cells, by the same route or a different route, a T-cell growth factor that promotes the growth and activation of the autologous T-cells, or (b) autologous T-cells, which have been previously isolated, selected for highly avid recognition of an antigen of the cancer, the regression of which is to be promoted, modified to express a T-cell growth factor that promotes the growth and activation of the autologous T-cells, and rapidly expanded in vitro only once, whereupon the regression of the cancer in the mammal is promoted.
EP2519102A2 NOVEL PYRIMIDINE COMPOUNDS AS mTOR AND PI3K INHIBITORS The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.
US20080287544 Method for Screening Substance by Measuring PPAR DELTA Activating Effect and Agent The present invention provides a method for screening a substance having a thermogenesis enhancing effect containing a compound having an effect activating PPARδ, an agent containing the compound, and an agent having antidiabetic, antiobestic or visceral accumulated fat-lowering function. The present invention provides an agent containing a compound having an effect activating PPARδ, which is a peroxisome proliferator activated receptor, and having effects which enhances nonshivering thermogenesis (nST), specifically enhances uncoupling respiration in mitochondria of cells in an adipose tissue or the like, or proton leak in inner membranes of mitochondria, and increases the amount of expression of UCP1, and provides an antidiabetic agent, an antiobestic gent and a visceral accumulated fat-lowering agent containing the compound. Further, the present invention provides a method for screening the compound by measuring a PPARδ activating effect.
CN101744861A Plaster for treating hyperostosis The invention discloses a plaster for treating hyperostosis, relating to a plaster for treating diseases, such as hyperostosis, cervical spondylopathy, lumbar disc herniation, and the like. The plaster is mainly prepared in order to solve the problems of poor treating effect and long course of treatment of the existing plaster for treating hyperostosis. The plaster is prepared by safflower, scorpion, frankincense, myrrh, cinnabar, periostracum cicadae and red iron oxide. The plaster has good treating effect and short course of treatment in treating hyperostosis, cervical spondylopathy, lumbar disc herniation, scapulohumeral periarthritis, strain of lumbar muscles, joint swelling and pain, and the like. The acute disease can be cured by one plaster, and the chronic disease can be cured by 3-4 plasters.
EP1615634B1 Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists This invention generally relates to derivatives of substituted azabicyclo hexanes of formula I. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.
CN103301474A Usage and related drugs of human RNF40 gene The invention discloses usage and related drugs of human RNF40 gene and specifically discloses usage of human RNF40 gene in tumor treatment and drug preparation. The invention further provides an oligonucleotide molecule separated from the human RNF40 gene, a human RNF40 gene interference lentivirus carrier, human RNF40 gene interference lentivirus and usage thereof. The oligonucleotide molecule or the lentivirus carrier containing the oligonucleotide molecule sequence and lentivirus provided by the invention can specifically inhibit the expression of the human RNF40 gene, and particularly the lentivirus can efficiently infect target cells and effectively inhibit the expression of RNF40 gene in the target cells so as to inhibit the growth of tumor cells and promote the apoptosis of the tumor cells, thereby having important significance in tumor therapy.
CN101265212B Antineoplastic alkanna tinctoria ketoximes derivatives The invention discloses lithospermum ketoxime derivant which can be used for resisting tumour in the technology field of medicine. The lithospermum ketoxime derivant is 5, 8-dimethoxy-1, 4-naphthoquinone derivant which is replaced by 6-, and has the following structural formula, wherein, R is alkyl and aralkyl. The lithospermum ketoxime derivant is synthesized, and the antitumor activity thereof is measured; alkannin is structurally modified and reorganized, so that an antitumor compound with lowered toxicity and increased water-solubility is obtained.
US20110046086 Composition Comprising Polysaccharide Extracted from Panax Ginseng Preventing and Treating Liver Diseases The present disclosure relates to a Panax ginseng polysaccharide extract, which is useful for liver protection or for the prevention and treatment of liver diseases, and a method for preparing the same. Further, the present invention relates to a composition for the prevention and treatment of liver diseases, comprising the Panax ginseng polysaccharide extract as an active ingredient, and a food composition comprising the same.
CN102319222A Decitabine freeze-dried preparation and preparation method thereof The invention provides a Decitabine freeze-dried preparation and a preparation method thereof. The solution before being subject to freeze-drying process comprises Decitabine, organic solvent, pH regulator, and water for injection. The preparation method comprises the following steps: uniformly dispersing Decitabine in the organic solvent, putting the mixture in a 0-10 DEG C solution of water forinjection dissolving the pH regulator to dissolve Decitabine completely, so as to let the organic solvent account for 0.3-4.0 % of the total volume of the final mixture; then filtering, degerming, carrying out split charging in glass bottles, carrying out freeze drying to remove the organic solvent and the water for injection, so as to obtain the Decitabine freeze-dried preparation for clinical use. According to the invention, in the freeze-dried preparation, the content of the organic solvent residues is less than 0.8%, the preparation process is simple and convenient, the production steps are easy to control, the pollution to production equipment and environment caused by the organic solvent is reduced, and the product quality is guaranteed.
US20080050451 Methods for assessing dehydration and shock, assays and kits for the methods The present invention is in the medical and consumer arenas. The invention presents the use of a salivary amylase assay to diagnose, quantify, and monitor the hydration status, the onset and progress of shock in an animal that produces salivary amylase, such as a human. The assay tests the saliva sample from the animal. Test kits and assays for such use are also presented.
WO2008118883A1 Administering antisense oligonucleotides complementary to human apolipoprotein b Methods for long-term lowering of lipid levels in human subjects and for the treatment of conditions associated with elevated LDL-cholesterol and elevated ApoB are provided.
US20090012056 Quinoline Compounds Capable of Binding the Cb2 and/or the 5-Ht6 Receptor The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess antagonist potency for the 5-HT6 receptor and/or are capable of selectively modulating the cannabinoid 2 receptor: and the use of such compounds or pharmaceutical compositions thereof in the treatment of CNS disorders.
CA2387727C Benzopyranyl guanidine derivatives, process for preparation thereof, and pharmaceutical compositions containing them The present invention relates to novel benzopyranyl guanidine derivatives of formula (1), wherein R1, R2, R3, R4, R5, R6, n and * are each defined in specification, process for preparation thereof and pharmaceutical use of the benzopyranyl guanidine derivatives. The benzopyranyl guanidine derivatives of the present invention can be used for protecting heart, neuronal cell or brain damage, preserving organs, and also the benzopyranyl guanidine derivatives are pharmacologically useful for inhibiting NO generation, and for suppressing lipid peroxidation, angiogenesis or restenosis.
EP1549314B1 Use of brimonidine in the treatment of dementia and parkinsons disease Methods of preventing or retarding the degeneration of neurons and/or methods for treating Alzheimer's disease or Parkinson's disease, comprising administering a therapeutically effective amount of brimonidine.
EP2483271A1 Pyrazoline dione derivatives as nadph oxidase inhibitors The present invention is related to pyrazoline dione derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
US7528132 immunodeficiencies, cancers, cardiovascular diseases, endocrine disorders, Parkinson's disease, metabolic diseases, tumorigenesis, Alzheimer's disease, heart disease, diabetes, neurodegeneration, inflammation, kidney disease, atherosclerosis and airway disease; indazolyl [1,2,4]triazine compounds A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as immunodeficiencies, cancers, cardiovascular diseases, endocrine disorders, Parkinson's disease, metabolic diseases, tumorigenesis, Alzheimer's disease, heart disease, diabetes, neurodegeneration, inflammation, kidney disease, atherosclerosis and airway disease.
CN103083296A Application of salvianolic acid A composition in preparing medicines for protecting cerebrovascular endothelial cells Application of salvianolic acid A composition in preparing medicines for protecting cerebrovascular endothelial cellsThe invention relates to application of a salvianolic acid A composition for preparing medicines for protecting cerebrovascular endothelial cells. The composition is prepared from the following components in percentage by weight: 90-99% of salvianolic acid A, 0.1-3% of alkannic acid, 0.1-3% of rosmarinic acid, 0.1-3% of salvianolic acid B and 0.1-5% of salvianolic acid C.
CN101993448A Anti-mycobacteria oxazolidinones used for treating infectious disease The invention provides anti-mycobacteria oxazolidinones used for treating infectious disease. Concretely, the invention provides heterocycle oxazolidinones which is shown by the following formula I and can be taken as anti-mycobacteria drug, or pharmaceutically acceptable salt and prodrug thereof, or drug composition containing the heterocycle oxazolidinones, application method thereof and method for preparing the compounds.
EP1603557A4 Synthesis of peloruside a and analogs thereof for use as antitumor agents The present invention provides (+)- Peloruside A and analogs thereof having microtubule-stabilizing activity, and a process for synthesizing these compounds. Also provided are intermediates and a process for synthesizing thereof. These compounds exhibit antiproliferative activity and are useful for treating cancer.
US20050267022 Identification of novel factors that block programmed cell death or apoptosis by targeting JNK Methods and compositions for modulating apoptosis by acting on the c-Jun-N-terminal kinase (JNK) pathway and assays for the isolation of agents capable of modulating apoptosis, including modulators of the JNK pathway are disclosed. A method of modulating JNK pathway independent of Gadd46β is disclosed. Methods and compositions are presented for the preparation and use of novel therapeutic compositions for modulating diseases and conditions associated with elevated or decreased apoptosis.
WO2012012710A3 Radiation sensitization agents for prostate cancer Compositions and methods are provided for sensitizing neoplastic cells to radiotherapy. The invention provides aptamer-inhibitory nucleic acid chimeras that selectively inliibit the expression of radiosensitizing genes in neoplastic cells expressing a cell surface molecule that binds the aptamer.
CN101366810A Medicament composition for preventing birth defection and improving memory The invention relates to a medical composition for preventing birth defects and improving memory and intelligence, which comprises Langehead Atractylodes Rhizome, Gynostemma pentaphylla, vitamin A, beta carotene, vitamin B complex, vitamin C, vitamin D, vitamin E, and macroelements of calcium and magnesium. The medical composition is mainly suitable for pregestational women, pregnant women and wet nurses, is very effective in preventing the birth defects and improving the memory and the intelligence, has both health care and tonic efficacies, and does not generate any side effects even after long-term application.
EP2279180A1 PROCESS FOR PREPARING A CRYSTALLINE FORM COMPOUND OF 3-BENZYL-2-METHYL-2,3,3a,4,5,6,7,7a-OCTAHYDROBENZOÝd¨ISOXAZOL-4-ONE A process for preparing a crystalline form compound of 3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one is described, comprising the step of reacting 3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one with oxalic acid in one or more solvents, wherein at least one solvent is a solvent having a carbon atom number of from 3 to 6, said solvent being non-halogenated and having a dielectric constant ε within the range from 4 to 25. The process of the invention enables a co-crystal comprising 3-benzyl-2-methyl-2,3,3a,4,5,6,7, 7a-octahydrobenzo[d]isoxazol-4-one and oxalic acid to be obtained.
US20120121668 Compositions for oral adminstration of active principles requiring masking of taste A process for the preparation of a composition intended for the oral administration of active principles with unacceptable taste, which comprises from about 15% to about 30% of organoleptically unpleasant active ingredient (principle) that is mixed with from about 60% to about 80% of an ester of glycerol or of a fatty acid, to which a wax is optionally added and to which a surfactant is added, and in that it is prepared by a spray-cooling process which can produce a particle size of less than 350 μm.
CN103330708A Application of 5-(3', 5'-dimethoxybenzylidene)-2-sulfo-imidazole-4-one to preparation of drug for treating cerebrovascular disease The invention discloses application of 5-(3', 5'-dimethoxybenzylidene)-2-sulfo-imidazole-4-one to preparation of drugs for treating cerebrovascular diseases. According to relevant researches disclosed by the invention, the compound has a remarkable cerebral nerve protection effect, can obviously reduce the volume of cerebral infarction of a focal cerebral ischemia rat and can obviously improve neurological signs; and moreover, the protection effect of an IV4 compound to cerebral ischemic injuries is related to the inhibition of the activation of lysosomal enzyme cathepsin B, so that the compound can be used for preparing drugs for preventing or treating diseases such as ischemic brain injuries, cerebral hemorrhage, cerebral thrombosis, cerebral embolism, cerebral infarction, cerebral stroke, lacunar infarction, transient ischemia attacks, cerebral arteriosclerosis and diabetic cardiovascular complications.
WO2009128547A1 Gene expression inhibitor selective for matrix metalloproteinase-9 gene Disclosed are: an inhibitor of the expression of matrix metalloproteinase-9 gene; a therapeutic agent for a disease associated with matrix metalloproteinase-9; and a carcinostatic agent. Each of the agents comprises a pyrrole-imidazole polyamide having an N-methylpyrrole unit, an N-methylimidazole unit and a γ-aminobutyric acid unit. The pyrrole-imidazole polyamide can be folded at the site of the γ-aminobutyric acid unit to form a U-shaped conformation in a minor groove of a double-stranded domain comprising a part or the whole of a specific nucleotide sequence (SEQ ID NO:2, SEQ ID NO:4) included in a human matrix metalloproteinase-9 gene promoter and a strand complementary to the part or the whole of the specific nucleotide sequence. In the U-shaped conformation, a Py-Im pair, an Im/Py pair and a Py/Py pair in the pyrrole-imidazole polyamide target a C-G base pair, a G-C base pair, and both of an A-T base pair and a T-A base pair in the minor groove, respectively.
US20050239051 Use of isogenic human cancer cells for high-throughput screening and drug discovery A strategy for drug-screening is based on cells that are isogenic except for a gene of interest. Each cell can be tranfected with a vector that encodes a different fluorescent protein that can be differentially detected to monitor cell growth. Co-culture of both cells allows facile screening for compounds with selective toxicity towards a gene of interest. The drug screening is broadly applicable for mining therapeutic agents targeted to specific genetic alterations responsible for cancer development.
US20100076094 Formulation containing phosphate derivatives of electron transfer agents There is provided an emulsion composition for therapeutic administration comprising: (a) at least one mono-(electron transfer agent) phosphate derivative; (b) at least one di-electron transfer agent phosphate derivative; wherein the amount of transfer agent phosphate derivatives is no less than equimolar to the amount of di-electron transfer agent phosphate; and (c) a suitable carrier.
WO2007148631A1 Composition for promoting the production of equol The object is to provide a composition which can significantly promote the production of an equol. When added to a pharmaceutical agent or a beverage/food, the composition can exerts an effect of preventing a vascular disease because of its cholesterol level-lowering effect, an effect of preventing breast cancer or prostate cancer, and an effect of preventing and/or treating osteoporosis. When added to an animal feedstuff or a pet food, the composition can exert an effect of increasing the bone density to thereby prevent the leg weakness in pigs, strengthen an egg shell in egg-laying chickens, and prevent osteoporosis in dogs or the like. Thus, disclosed are: a composition comprising lactobionic acid, a salt thereof or lactobionolactone as an active ingredient; and a beverage/food, animal feedstuff, pet food or a pharmaceutical agent comprising the composition and having an effect of preventing or treating osteoporosis, an effect of increasing the bone density, an effect of preventing breast/prostate cancer, and an effect of lowering the cholesterol level.
US20100069323 Composition for application to skin or mucosa Disclosed is a composition for application to skin or mucosa comprising alginic acid and/or salts thereof, which has reduced cytotoxicity against a skin cell or mucosa cell and higher safety, the composition for application to skin or mucosa comprises an alginic acid and/or salts thereof that contains substantially no low-molecular-weight fraction having a molecular weight of 3,500 or less.
US20080279940 For treatment or prevention of chronic pain The present invention relates to a novel spontaneously dispersible pharmaceutical composition, e.g. a microemulsion preconcentrate, in which the active drug substance is a cannabinoid receptor binding compound, in particular a corresponding naphthalene derivative, that is useful, e.g., for the treatment or prevention of chronic pain.
US7060732 Antiacne; skin disorders; packaged separately Two separate compositions, one containing an effective anti-acne treating amount of a first active ingredient and one containing a second active ingredient that is incompatible with the first active ingredient are packaged within and dispensed from a common dispenser. By packaging these two active ingredients in this manner, long shelflife and convenient dispensing and application are provided.
US20080057115 2-propyloctanoic acid for treating neurodegenerative diseses contained in a capsule, internally taken safely without feeling acidness, pain, burning sensation in the oral cavity, dissoved quickly in stomach without delay; shell comprises gelatin, sacchride as base and glycerine as plasticizer, a fat The present invention relates to a soft capsule which is easily disintegrated in the stomach, wherein the contents thereof are not easily leaked at the time of mastication, which is obtained by providing a soft capsule comprising (2R)-2-propyloctanoic acid or a salt thereof with at least one property, preferably all properties, selected from (A) wherein it has a strength of 150 to 400 N by a cracking test; (B) wherein it has a disintegration time of 3 to 10 minutes by the disintegration test stipulated in Japanese Pharmacopoeia; (C) wherein the capsule shell has a shell thickness of 0.05 to 0.50 mm; (D) wherein the capsule shell has a first seam thickness of 0.10 to 0.55 mm; (E) wherein the capsule shell has a second seam thickness of 0.05 to 0.50 mm; (F) wherein the capsule shell has a water content of 5.0 to 9.0%.
US8377483 Bioactivation of iron salt, especially an ferric ferrous salt, by adding a magnesium salt (MgCl2); useful as a medicine to treat diseases such as diabetes, freshness preservative agent, and animal and plant growth promoter The object of the present invention is to stabilize bioactivation of iron salt. Said object is attained by adding a magnesium salt to said iron salt. Said iron salt stabilized by said magnesium salt is useful as medicine to treat incurable diseases such as diabetes and growth promoting agent of animals and plants.
US20080020014 Implantable devices containing nuclear receptor ligands for the treatment of vascular and related disorders The present invention is directed to implantable devices (e.g., drug-delivery stents) containing nuclear receptor ligands. The nuclear receptor ligands may be, inter alia, PPAR ligands or retinoids. The invention also provides for a method of treating or preventing vascular disorders (e.g., restenosis) and related disorders using the nuclear receptor ligand-containing devices.
CN101229157A Calldesartan ci1exetil medicine compounds The invention discloses a candesartan ester drug composition which consists of candesartan ester and phospholipids; wherein, the weight of the phospholipid is 0.5 to 10 times that of the candesartan ester; the composition of the invention inserts or wraps the candesartan ester into a central hydrophobic layer of a bimolecular layer of the phospholipid to prepare the candesartan into a candesartan ester liposome composition and the candesartan ester can be prepared into candesartan preparations with suitable pharmaceutical excipient. The composition can prevent the decomposition of the candesartan ester and keep long stability of the candesartan ester so as to prolong the period of validity of the candesartan ester preparations.
EP1848455A1 Use of calcitonin and calcitonin-like peptides to treat and prevent multiple sclerosis Methods for treating and preventing multiple sclerosis by administering to a patient an effective amount of calcitonin, calcitonin-like peptides or calcitonin mimetics to a patient. Additionally, 1,25-dihydroxyvitamin D analogs can be used in combination with the calcitonin, calcitonin-like peptides or calcitonin mimetics.
CN101153023A Tetrahydrochysene isoquinoline derivant, its producing method and uses of the same The present invention relates to the field of medicinal chemistry, and specifically relates to a category of novel tetrahydrocannabinol isoquinoline compounds (I), the preparation method, the pharmaceutical preparations containing the compounds and the application as tumor multi-drug and drug-resistant reversal agents. Wherein, the R 1 , R 2 and X are defined in the specification.
WO2010085753A1 Rosacea treatments and kits for performing them Regimen for the treatment of rosacea include the application of an anti- redness composition to at least a portion of the cleansed area of skin afflicted with rosacea. The regimen may include the application of one or more of a polymetal complex, a composition containing metronidazole, and/or a protective composition. Kits containing components useful in performing such regimens are also described.
US20110166218 Methods for micronization of hydrophobic drugs The invention involves methods and products related to the micronization of hydrophobic drugs. A method of micronizing hydrophobic drugs using a set of solutions including an aqueous solution is provided. The invention also relates to products of micronized hydrophobic drugs and related methods of use.
US7122687 Sodium salt formation of Mycophenolic acid In one aspect, the present invention provides a process for producing a sodium salt of an immunosupressant of Formula I
CN102327233A Dimercaptosuccinic acid granular formulation The invention provides dimercaptosuccinic acid solid preparations, in particular to a dimercaptosuccinic acid granular formulation, which is prepared from dimercaptosuccinic acid and auxiliary materials, wherein the auxiliary materials are taste-masking preparation and one kind or more than two kinds of the following materials which are selected from the following groups: diluent, disintegrating agent, suspending agent, sweetener and bonding agent. The dimercaptosuccinic acid granular formulation is characterized in that the taste-masking preparation is beta-cyclodextrin and liquid cream flavor essence, and is prepared into the granular formulation through the following method: after the dimercaptosuccinic acid and the liquid cream flavor essence are mixed, and then the beta-cyclodextrin is added to be uniformly mixed. The dimercaptosuccinic acid granular formulation adopts the novel taste-masking technology, the garlic like smell of the dimercaptosuccinic acid is effectively masked, and meanwhile, the formulation has the pleasant fragrance and fruity taste, and is more suitable for children to take.
WO2012129914A1 3-amino-2-hydroxy-4-phenyl-valyl-isoleucine and preparation method and use thereof The present invention relates to a new compound, 3-amino-2-hydroxy-4-phenyl-valyl-isoleucine, of the structural formula: and the compound is produced by the fermentation of Streptomyces parvus CGMCC No. 4027, has an inhibitory effect on aminopeptidase and can be used to prepare an aminopeptidase inhibitor drug.
US6943174 6,5-Fused bicyclic heterocycles The present invention provides compounds of Formula (I) wherein Q1, Q2, Q3, Q4, Y1, Y2, and Z are as defined in the description, and pharmaceutically acceptable salts thereof, and C1-C8 alkyl esters thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of Formula (I) and their pharmaceuticalyl acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.
CN101874785A Recipe of valnemulin hydrochloride enteric-coated pellet and preparation method thereof The invention provides a recipe of a valnemulin hydrochloride enteric-coated pellet and a preparation method thereof, wherein, acrylic resin water dispersion is taken as coating liquid, and water is taken as a solvent, thus changing the method that the existing resin coating liquid selects high concentration alcohol as the solvent, lowering cost and overcoming the defect of environmental influence due to evaporation of a large amount of alcohol during the coating process. The preparation method of the valnemulin hydrochloride enteric-coated pellet comprises the steps of preparation of the valnemulin hydrochloride medicine carrying pellet, preparation of the coating liquid and preparation of valnemulin hydrochloride coating. By adopting an extrusion-spheronization process procedure, the preparation method solves the defects of a one-step fluidized bed granulating method such as coarse and loose particles, large particle size range, a large amount of dust; and the pellet prepared by the method has even particle size and narrower distribution range, thus being beneficial to uniform saturation of the coating liquid on the particles, and improving the taste masking effect.
CN102813646A Application of homomangiferin in preparing pharmaceuticals for preventing senile dementia and hypomnesis, homomangiferin pharmaceutical compositions and homomangiferin preparations The invention discloses application of homomangiferin in preparing pharmaceuticals for preventing senile dementia and hypomnesis. Researches shows that homomangiferin can improve damaged learning and memory ability of APP (amyloid protein precursor) transgenic mice evidently, and can improve relatively-long-term memory in short-term memory of the APP transgenic mice. The homomangiferin can increase content of Ach (acetylcholine), improve activity of CHAT (choline acetyl transferase) and inhibit activity of AchE (acetylcholinesterase), and accordingly indexes in terms of APP transgenic dementia model pathology, cholinergic system, cell apoptosis and the like can be improved. The homomangiferin and homomangiferin compositions can be used for preparing pharmaceuticals for preventing senile dementia and hypomnesis.
US20120201870 Dicalcium Phosphate Ceramics, Dicalcium Phosphate/Hydroxyapatite Biphasic Ceramics and Method of Manufacturing the Same The present invention discloses a method of manufacturing pure dicalcium phosphate ceramics or dicalcium phosphate/hydroxyapaite (HA) biphasic ceramics for medical applications in hard tissue areas to be used as implant materials. These ceramic implant materials are in granular form or in block form, and are prepared by using an acidic phosphate compound, a basic calcium phosphate compound comprising HA, and water. The dicalcium phosphate ceramic comprises either dicalcium phosphate dihydrate (CaHPO4.2H2O, DCPD) or dicalcium anhydrous (CaHPO4, DCPA). Wherein, when the acidic phosphate compound is provided in an amount stoichiometrically equal to or in excess relative to the basic calcium phosphate compound, a reaction product is the DCPD or DCPA ceramic; when the acidic phosphate compound is provided in the amount stoichiometrically less than the basic calcium phosphate compound, the reaction product is the DCPD/HA or DCPA/HA biphasic ceramic.
CN102048754B Compound arsenic acid preparation capable of reducing toxicity of arsenic The invention discloses a compound arsenic acid preparation capable of reducing the toxicity of arsenic and relates to a compound arsenic acid preparation containing arsenic trioxide. The compound arsenic acid preparation can be used for solving the problem that the exiting arsenic acid medicament has great toxicity. The compound arsenic acid preparation capable of reducing the toxicity of the arsenic comprises the arsenic trioxide, cimifugin and solvent. The compound arsenic acid preparation capable of reducing the toxicity of the arsenic can reduce the toxicity of the arsenic trioxide, reduce the damages to normal cells, tissues, organs and organisms and have no influence on the treatment effect of arsenic acid on cancer cells.
CN101982195A Medicine for treating rheumatoid arthritis pain and preparation method thereof The invention discloses a medicine for treating rheumatoid arthritis pain, which comprises the following raw materials of ailanthus twig, willow twig, mulberry twig, elm twig, peach twig, dahurian angelicaroot, angelica, red peony root, radix scrophularia, dried rehmannia root, cassia, rhubarb, semen momordicae, frankincense, myrrh, Chinese asafoetida, liquorice, rhizoma curcumae longae, rehmanniae vaporata, Szechuan lovage rhizome, radix angelicae pubescentis, achyranthes root, cortex acanthopanacis, garden burnet root, trogopterus dung, zedoary, manchurian wildginger, pinellia tuber, siberian cocklour fruit, notoginseng, common clubmoss herb, raidx astragali, divaricate saposhnikovia root and minium. The preparation method comprises the following steps: adding 5000g of sesame oil to a pot for heating to 40 DEG C; sequentially adding the raw materials to the pot for heating to 100 DEG C and keeping the temperature for 30 minutes; filtering out dregs; adding the obtained liquid medicine to the pot for heating to 100 DEG C and keeping the temperature for 30 minutes; concentrating to obtain paste; canning and sealing after being cooled; and storing in a crypt for 30 days for use. The invention has the advantages of simple preparation process, convenient use, good treatment effect, addressing both the symptoms and root causes, no side effect, low cost, short treatment course and certain efficacy on treating rheumatoid arthritis pain.
WO2014067986A1 Galactoside inhibitor of galectin-3 and its use for treating pulmonary fibrosis The present invention relates to a compound of the general formula (I) for pulmonary administration. The compound of formula (I) is suitable for treating pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a mammal. Furthermore the present invention concerns a method for treatment of pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a human subject.
US20110009482 Methods of treating copd Disclosed is a method of treating chronic obstructive disease, said method comprising administering an effective amount of a CXCR2 antagonist and administering an effective amount of at least one drug selected from the group consisting of: angiotensin-converting enzyme inhibitors, Angiotensin II receptor antagonists, cardioselective beta blockers, and lipid regulating drugs. Examples of the CXCR2 antagonist include: (formula 1.0A and 1.0B).
CN1569861A Pharmaceutical acid addition salt of adefovir dipivoxil and its pharmaceutical use The invention discloses four pharmaceutical acid addition salts of adefovir dipivoxil, including aspartic acid adefovir dipivoxil ester salt, taurine adefovir dipivoxil ester salt, gluconic acid adefovir dipivoxil ester salt, fructose adefovir dipivoxil and their pharmaceutical use.
CN101991564A Production process for separating, extracting and purifying bioactive substance calcium nervonate and application thereof to treatment of Alzheimer's disease The invention relates to a process flow for separating, extracting and purifying bioactive substance calcium nervonate. The process flow comprises the following steps of: directly extracting smashed oil nuts by using carbon dioxide (CO2) supercritical equipment in the presence of an entrainer to obtain a nervonic acid derivative crude product; and then adding calcium hydroxide to perform saponification reaction, separation, purification, crystallization and drying to obtain an extremely pure calcium nervonate product. The process flow has the advantages of simple process, environmental friendliness, low operation temperature, high purity of active ingredient calcium nervonate, high yield, low cost, obvious market competition advantage and the like, so that the process flow is adopted by Hangzhou Saweitan Biotechnology Company Limited for industrialized production. The bioactive substance calcium nervonate of the invention can be mixed with pharmaceutically applicable carriers and prepared into various formulations for treating the Alzheimer's disease.
CN1596885A Propyl gallate freeze-dried powder-injection and its preparation method A freeze-dried powder injection of gallopropylate is prepared from gallopropylate, cosolvent chosen from dextran, cyclodextrin, and polysorbate 80, and freeze-drying supporting agent chosen from detran, mannitol, glucose, lactose and sodium chloride.
WO2007079000A2 Kit comprising an osmotic laxative and a stimulant laxative for prepariing the colon for virtual colonoscopy An osmotic laxative followed by a bowel movement, followed by a stimulant laxative produces safe and effective cleansing of the colon with a minimal volume of liquid remaining in the colon in preparation for visualizing the interior of the colon by virtual colonoscopy. Administering to a patient a reduced volume of a PEG in water solution followed by an oral stimulant laxative, such as bisacodyl, after a biologically determined interval, cleanses the colon in preparation for virtual colonoscopy, without the profuse uncontrollable diarrhea that typically follows either ingestion of large volume isotonic lavages, or smaller volume hypertonic lavages.
WO2008102584A1 Novel flavanol compound and method for production thereof Disclosed is a novel compound which can be used as a pharmaceutical agent, a cosmetic, a health food, a food additive or the like. Specifically disclosed is a flavanol compound shown by the formula (1). (1)
CN101007003A A stable torasemide injection and its preparation method There is provided an injection with torasemide as the main active ingredient in the invention, the preparing method of the injection is also included in the invention. The stability of the injection in the invention has been greatly improved. There is solubilizing agent and stabilizer in the preparation, the pH value is 9.0 or larger. The preparing method includes the following steps: adding 1-50% (by weight) of solubilizing agent to certain amount of injecting water; adding torasemide to the water, after it is completely dissolved, adding 0.1-5% part of stabilizer; adding water to requested amount and stirring uniformly; adding activated char to adsorb for 30min at high temperature; decarbonizing and filtering; adding medically used alkali to regulate the ph value to 9.0 or larger; aseptically filtering; after the assay is approved, packaging, degerming and stocking. The advantages of the invention include: high stability, short preparing time, low cost, no haemolyticus, blood vessel stimulus and allerfic response, low growing speed of relative substances.
EP2105143A1 Pharmaceutical compositions based on salts of tiotropium and ciclesonide A medicament (A) comprises a combination of anticholinergic agent(s) (I) and the corticosteroid ST-126 (II), optionally together with pharmaceutical auxiliaries. - ACTIVITY : Antiinflammatory; Antiasthmatic; Antiallergic. - MECHANISM OF ACTION : Anticholinergic.
US20050003000 Method for the the formation of ibuprofen crystals The present invention relates to a process for the formation of profen crystals, which comprises carrying out the formation of solids by displacement precipitation, cooling crystallization, evaporative crystallization or a combination thereof in the presence of one or more additives, and the use of the profens thus prepared for pharmaceutical formulations.
US20120070409 Tetracyclic fused heterocyclic compound and use thereof as hcv polymerase inhibitor The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
US20070043018 2"-Hydroxynicotianamine, process for producing the same and angiotensin converting enzyme inhibitor, hypotensive drug and health food The invention provides 2″-hydroxynicotianamine; a method for producing 2″-hydroxynicotianamine comprising the step of obtaining an extract solution from a buckwheat sample followed by obtaining a fraction having an inhibitory activity for the angiotensin-converting enzyme by ion-exchange chromatography using an anion exchange resin; novel substances having an ACE inhibitory activity by preparing an inhibitor for the angiotensin-converting enzyme, a vasodepressor agent and a health food each containing 2″-hydroxynicotianamine; methods for producing the novel substances; an inhibitor for the angiotensin-converting enzyme and a vasodepressor agent having the novel substance as an effective ingredient; and a health food containing the novel substance.
US20100216877 Storage Stable Prostaglandin Product A prostaglandin composition comprising prostaglandin and a low-density polyethylene container are disclosed. The prostaglandin compositions are stable in polyethylene containers over longer period of time.
CN103524448A Enrofloxacin-saccharin compound The invention discloses an enrofloxacin-saccharin compound as well as a preparation method thereof, and belongs to the field of veterinary drugs. The enrofloxacin-saccharin compound is mainly prepared from the following raw materials in parts by weight: 35-65 parts of enrofloxacin and 35-65 parts of sodium saccharin. The enrofloxacin-saccharin compound is prepared by the following steps of firstly dissolving sodium saccharin into water, adding hydrochloric acid, and crystallizing saccharin, thereby obtaining purified saccharin; then dissolving enrofloxacin into an alcohol solution; adding purified saccharin, carrying out ultrasonic treatment in a water bath, reacting enrofloxacin and saccharin, and spray-drying, thereby obtaining the enrofloxacin-saccharin compound. The prepared enrofloxacin-saccharin compound not only effectively removes bitterness of enrofloxacin, but also improves the solubility of enrofloxacin in water, so that the bioavailability of enrofloxacin is improved, and further the curative effect of enrofloxacin is improved. Compared with the prior art, the production method saves time, is high in yield, and is suitable for industrial production.
EP0918754B1 Anthranilic acid diamides derivatives, their preparation and pharmaceutical use as anti-gastrin agents Compounds which can be represented by general formula (I) indicated below, and in which the anthranilic acid aromatic ring may be mono- or di-substituted by the R1 group which can be selected independently from hydrogen, methyl and chloro, and in which the substituents at the chiral centre (marked with an asterik in formula (I)) have the R (Rectus) configuration.
EP2638005A2 S-t-butyl protected cysteine di-peptide analogs and related compounds S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).
CN1566092A Indene ketone diindyl class compound, preparation method and medical use thereof The invention discloses a category of indene ketone and indoles compound, its preparing process and medical use thereof, wherein R1, R2 is H, OH, C1-C4 alkoxy, C1-C6 alkoxy, -OCOAr (Ar isphenyl or replaced phenyl), R3 is piperidine, pyrrolidine, methyl pyrrolidine, morpholine, dimethylamino, diethylamino, diisopropyl amino, methylene imino, n=2 or 3. The compounds has high appetency with female hormone acceptor after being screened.
WO2014105666A1 Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties Disclosed are compounds of Formula Gl (structurally represented): where "RG3" "Rd1" to "Rd4", "n", "m", "p", "W", "X", "Y", and "Z" are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
CN1883464A Ophthalmic preparation containing sodium new houttuyfonate The invention relates to an eye preparation containing sodium new houttuyfonate and process for preparation, wherein the preparation comprises sodium new houttuyfonate as the active constituent and pharmaceutically acceptable auxiliary materials, and can be prepared into various eye preparations including eye drops, gels, turbid liquors, microspheres, microemulsions, implants and effervescent tablets.
US20100016377 Use of a p38 Kinase Inhibitor for Treating Psychiatric Disorders The use of 6-(S-Cyclopropylcarbamoyl-S-fluoro-2-methyl-phenyl)-N-(2,2-dimethylproyl)-nicotinamide, which is known in the art as a p38 kinase inhibitor in the treatment or prophlaxis of one or more psychiatric disorders.
CN101289477A N-phenylpropenoyl chitosan oligosaccharide and preparation thereof The invention relates to chito-oligosaccharide, in particular to an N-benzene acryloyl chito-oligosaccharide and the preparation thereof; wherein, the chito-oligosaccharide is provided with mixed components with the average molecular weight from 800 to 6000 and the degree of deacetylation from 80 to 100 percent; the degree of substitution of the benzene acryloyl is from 30 to 100 percent; the general structure formula of the components is provided as follows, the chito-oligosaccharide has the effects of lowering the blood fat and blood glucose, enhancing the immune function, inhibiting the tumor and fighting against the fatigue and delaying the aging as well as alleviating the analgesia, diminishing the inflammation and the effects of anti liver virus, anti snake venom, etc., and can be served as the important raw material for certain medicines, health food and cosmetics.
US20110237615 Narcotic Drug Formulations with Decreased Abuse Potential The present application relates to novel narcotic formulations having a decreased injection abuse potential In a representative embodiment, the formulation comprises methadone hydrochloride (6-dimethylamino-4,4-diphenylheptan-3-one, a synthetic opiod), meglumine, cellulose, lactose, and magnesium stearate The application further illustrates methods for making the contemplated formulations.
WO2010005087A1 Amidine derivative Disclosed is a novel amidine derivative having an inhibitory activity on activated blood coagulation factor-X or a pharmaceutically acceptable salt thereof. Specifically disclosed is a compound represented by formula (I) [wherein each symbol is as defined in the description] or a pharmaceutically acceptable salt thereof.
WO2010141550A3 11beta-hydroxysteroid dehydrogenase type 1 (11-beta hsd1) inhibitors This invention features a chemical entity E, which is a compound of Formula I, or a salt (e.g., a pharmaceutically acceptable salt), or an N-oxide thereof (e.g., a compound of Formula I, or a pharmaceutically acceptable salt thereof). Formula I is provided below: formula (I) R1, R2, R3, R4, R5, R6, R7, R8, R9, and A can be as defined anywhere herein.
US7772226 such as 3-(2-Butynyl)-2-(piperazin-1-yl)-3,5-dihydroimidazo[4,5-d]pyridazin-4-one trifluoroacetate, used as dipeptidyl peptidase-IV (DPPIV) inhibitors for the treatment of obesity and diabetes The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.
WO2013170379A1 Drug delivery across the blood-brain barrier using magnetically heatable entities It has been discovered that compositions comprising magnetically heatable entities (MHEs), therapeutic agents and optional carriers such as hydrogels can be piloted from an injection point in a blood vessel to a specific location of the blood-brain barrier (BBB) using for example, a magnetic resonance imaging (MRI) device for propelling, steering and tracking of MHEs. Once the MHEs have reached their target location at or near the desired blood vessel of the BBB, an alternating magnetic field causes the MHEs to controllably heat up, thereby reversibly increasing the permeability of the BBB and allowing the therapeutic (or cytotoxic) agent to enter brain tissue.
US20110158917 Anti-viral tissue product with visual efficacy indicator Anti-viral tissues are provided with a pH indicator which can communicate to a tissue user by means of visual indicia, via color changes, that the tissue has active ingredients. Furthermore, the pH indicators can be used to illustrate neutralization of the pH of infected nasal discharge, which has a higher pH than healthy nasal discharge, giving the user a reason to believe that the product is working to deactivate virus.
EP1325000B1 A thiazolidinedione derivative and its use as antidiabetic A compound 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione potassium salt or a pharmaceutically acceptable solvate thereof, a pharmaceutical composition containing such a compound and the use of such a compound in medicine, particularly in the treatment of diabetes mellitus.
US20100119590 Method of drug loading in liposomes by gradient A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.
US20130005741 Substituted pyrimidine as a prostaglandin d2 receptor antagonist The present invention is directed to a 2,6-substituted-4-monosubstitutedamino-pyrimidine compound of formula (I): or an enantiomer thereof, or an ester prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound.
CN1565441B Use of levobutylphthalide in prevention and cure of dementia The invention discloses the use of levogyration n-butyl benzene phthaleins in preparing medicament for preventing and treating aphrenia, in particular Hammer disease and blood vessel aphrenia.
EP1810683A1 Immunopotentiator and method and apparatus for producing the same An immunopotentiator to be used for enhancing an immune function of suppressing the proliferation of allogeneic tumor, the immunopotentiator containing, as an active ingredient, electrolyzed weakly alkaline water produced by electrolysis of water containing a silver component
CN101199513A Method of forming indole framework compound by catalysis reaction and application in anti-cancer medicament The invention discloses a forming method of a compound with indole architecture, comprising a catalytic reaction. The catalytic reaction is that at least one kind of lewis acid is used to catalyze Alpha and Beta unsaturated ketones and indole or derivatives of the indole to react, or to catalyze Alpha and Beta unsaturated aldehydes and the indole or the derivatives of the indole to react. The lewis acid comprises one of the following ethnic groups : metal halide, halogen, inorganic ammonium salts and organic sulfonic acid (salt). On the other hand, the invention also discloses an application of the compound with 3- indole architecture to the anticancer drugs.
US20080033003 Camptothecins Conjugated in Position 7 to Cyclic Peptides as Cytostatic Agents Compounds of Formula (I) are described in which the R1 group is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
CN103263430A Application of polyflavanostilbene A in preparation of medicaments for treating lung cancer The invention discloses an application of polyflavanostilbene A in preparation of medicaments for treating lung cancer. The compound shows good anti-lung cancer activity, can be used for preparing anti-lung cancer medicaments and belongs to the technical field of new uses of the medicaments. The polyflavanostilbene A can significantly inhibit non-small cell lung cancer cells A549, large cell lung cancer cells NCI-H460, lung squamous carcinoma cells HTB-8 and human lung squamous cell carcinoma cells QG-5, which are cultured in vitro, realize a smaller inhibition effect against human normal liver cells LO2 and peripheral blood lymphocytes and show obvious selectivity. The use of the polyflavanostilbene A in the preparation of the medicaments for treating the lung cancer, disclosed by the invention, belongs to the first disclosure, the framework type belongs to the brand new framework type, and the strong inhibition activity against the cells of the lung cancer is further unexpected.
CN102579457A Compound tetracaine composition as well as preparation method and application thereof The invention relates to a compound tetracaine composition as well as a preparation method and application thereof. The composition comprises the following raw medicines: tetracaine, ephedrine, phenobarbital, diphenhydramine, hydrocortisone and borneol. The compound tetracaine composition has the effects of removing necrotic tissue and promoting granulation, clearing heat and relieving pain, diminishing inflammation and resisting infection and promoting wound healing and has obvious curative effects of treating acute-stage anal fissure and acute attack of chronic anal fissure. When the compound tetracaine composition is matched with an anus suppository to perform non-surgical treatment of piles, the curative effects of the compound tetracaine composition on relieving bleeding, pain and abjection symptoms of piles are obvious. As a whole, the compound tetracaine composition has the advantages of obvious curative effect and the like, is quick to act, is convenient to use and is safe; and when the compound tetracaine composition is used, a patient does not feel pain; and effective rate reaches 100%.
CN103402987A 6-amino-2-phenylamino-1H-benzimidazole-5-carboxamide- derivatives and their use as microsomal prostaglandin E2 synthase-1 inhibitors This invention relates to compounds of formula (I) their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
CN102988783A Production method of gastrodin The invention discloses a production method of gastrodin. The production method comprises the following steps: smashing gastrodia elata tubers into fine blocks with the grain diameter smaller than 0.5-1.5cm; adding 80% alcohol with the weight as 2-4 times of gastrodia elata fine blocks, heating for extracting, controlling the temperature at 80 DEG C, controlling the time within 1 hour, and extracting for twice; filtering extractives, and combining filtrate; recovering alcohol from the filtrate in decompression mode, and concentrating to the concentration with the content of crude drug of 0.5g/ml, and obtaining gastrodin dry extract. The production method of gastrodin has the advantages of being high in utilization rate of effective ingredients, good in quality stability of products and low in production cost.
EP2069334B1 Aspalathin-like dihydrochalcone, extracts from unfermented rooibos and process for preparation The present invention relates to a novel chemical compound of the formula (I) and to pharmaceutically acceptable salts, derivatives and esters thereof. In addition, the invention also relates to a process for isolating the compound of the formula (I) from raw rooibos material. The present invention likewise relates to a rooibos extract which has a content of the compound of the formula (I) of at least 0.4% by weight. The invention further relates to the use of the chemical compound of the formula (I) and to the pharmaceutically acceptable salts, derivatives and esters thereof, and of the inventive rooibos extract as a medicament, especially for treatment of neurological and psychiatric disorders of the central nervous system. The expression “pharmaceutically active” also includes those effects which lead to a subjective improvement in mental state, in which case approval under pharmaceutical legislation need not be absolutely necessary. The compound of the formula (I) is shown below: (formula I).
CN103623182A Medicine for treating gynecological inflammations and preparation method thereof The invention discloses a medicine for treating gynecological inflammations and a preparation method thereof. The medicine is prepared from the following medicinal materials by weight: 5 to 20 parts of bone fossil of big mammals, 5 to 20 parts of Gorgon fruit, 3 to 10 parts of honeysuckle flower, 5 to 20 parts of dandelion, 3 to 10 parts of menthol, 3 to 10 parts of gingko, 5 to 20 parts of oyster, 5 to 20 parts of patrinia herb, 3 to 15 parts of wolfberry, 3 to 15 parts of white peony root, 3 to 15 parts of root of large-flowered skullcap, 5 to 20 parts of safflower, 3 to 15 parts of motherwort, 3 to 10 parts of spatholobus stem, 3 to 10 parts of Cherokee rose root, 3 to 10 parts of weeping forsythia capsule, 3 to 10 parts of aloe, 3 to 15 parts of Sichuan lovage rhizome and 5 to 20 parts of Chinese angelica. The medicine provided by the invention uses herbaceous plants as raw materials, has small toxic and side effects and is powder; the medicine is externally applied, can be rapidly dissolved and absorbed and has good anti-inflammation and sterilization effects and fast action.
US20090075964 Fragrance compositions and other compositions which contain naturally occurring substances found in corals This invention is generally related to the fields of fragrance compositions, personal care products, and home consumer products. This invention also relates to 20-pregnenes, in particular those found naturally occurring in corals and which affect mood in humans, to the incorporation of these 20-pregnene compounds into various compositions, and to methods of affecting the mood of individuals using such compounds.
CA2744428A1 Nutritional or dietary supplement composition and methods for using same for treating visual acuity loss This invention relates to nutritional or dietary supplement composition effective in the prevention, stabilization, reversal and/or treatment of visual acuity loss, namely reducing the risk of developing late stage or advanced AMD in people with early or intermediate AMD. The present invention also provides systems and methods for providing a nutritional or dietary supplement composition effective and safe for preventing, stabilizing, reversing and/or treating macular degeneration and/or visual acuity loss.
US20120003264 CDNA Corresponding to the Antigenome of Nonsegmented Negative Stranded RNA Viruses and Process for the Production of Such Viruses The present invention relates, in general, to a methodology for the generation of nonsegmented negative-strand RNA viruses (Pringle, 1991) from cloned deoxyribonucleic acid (cDNA). Such rescued viruses are suitable for use as vaccines, or alternatively, as plasmids in somatic gene therapy applications. The invention also relates to cDNA molecules suitable as tools in this methodology and to helper cell lines allowing the direct rescue of such viruses. Measles virus (MV) is used as a mode for other representatives of the Mononegavirales, in particular the family Paramyxoviridae.
US20080300201 Cell Cycle Arrest and Apoptosis The HIV-1 accessory gene vpr encodes a conserved 96-amino acid protein that is necessary and sufficient for the HIV-1-induced block of cellular proliferation and induction of apoptosis. Expression of vpr in CD4+ lymphocytes results in G2 arrest, followed by apoptosis. ATR, as a cellular factor that mediates Vpr-induced cell cycle arrest, is required for activation of the Breast Cancer-Associated Protein-1 (BRCA1). In addition, the Growth Arrest and DNA Damage protein (GADD45) is upregulated by Vpr in an ATR-dependent manner. Posttranscriptional silencing of either ATR or GADD45 leads to nearly complete suppression of the pro-apoptotic and/or cell cycle arrest effect of Vpr.
US20110091459 Imidazole modulators of muscarinic acetylcholine receptor m3 The present invention relates to new imidazole modulators of M3 muscarinic acetylcholine receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
CN103432556A Filler for gingival hemostasis The invention relates to filler for gingival hemostasis. The filler is prepared from the following substances in weight proportion: entada phaseoloides, physalis permviana, cortex ailanthi, fermented soybean, caltrop, malt, pawpaw, seville orange flower, China rose, chingma abutilon seed, hempleaf negundo chastetree leaf, anemonis raddeanae, papermulberry fruit, scaphium scaphigerum, nux prinsepiae, small centipeda herb, galanga galangal seed, bunge cherry seed, white hyacinth bean, butterflybush flower, flos daturae, cacumen biotae, pulsatilla chinensis regel, selaginella tamariscina, folium sennae, peucedanum decursivum maxim, cocklebur fruit, cicada slough, tangerine seed, astragalus complanatus, black soybean, panax japonicus, earthworm, dried ginger, hog brake, manchurian lilac bark, kapok, Chinese trumpet creeper, rhizoma dioscoreae hypoglaucae, large-leaved gentian, vermiculite schist seu, kamuning, dogbane leaf, cockscomb, divaricate saposhnikovia root, Japanese ardisia herb, potentilla discolor, scorpion, radix berberidis, stiff silkworm, radix polygonati officinalis and saffron. The filler for gingival hemostasis has the effects of strengthening teeth and regenerating gum and treating gingival bleeding to treat both symptoms and root causes, and can be used for effectively treating gingival bleeding, thus being suitable for clinical popularization.
CN101152152A Lgecycline composition for injection and processes for producing same The present invention relates to an injection igecycline combination and the preparing method. The combination comprises igecycline and antioxidant. The weight percentage of igecycline is 10 and the weight percentage of antioxidant is 0.01 to 10. The combination can also comprise 0 weight percent to 200 weight percent of excipient or 0 weight percent to 1 weight percent of chelating agent. Firstly excipient, antioxidant and chelating agent are weighed and taken according to a recipe quantity, and then injection water is added for melting. Igecycline is added according to the recipe quantity. Injection water is added to total content and is stirred to melt. The pH value is regulated between 7.0 and 9.0. Then 0.5 g per liter to 2 g per liter of medical solution bulk of needle carbon is added and is stirred at room temperature and is filtrated to eliminate carbon. A filtrate is rough filtrated and fine filtrated to remove bacteria. Content of the fine filtrated solution is mensurated and loading quantity is calculated according to labeled amount. Split charging, refrigeration and drying, vacuum capping and gland, the injection igecycline combination obtained. The injection igecycline combination is stable in quality, free of pollution, easy in operation storage and transport.
US20120264827 Sulfanylamide derivatives, uses thereof and compositions comprising them The present invention concerns a family of sulfanilamide derivatives of formula (I) as anticonvulsant agents, where R is selected from optionally substituted C4-C9 alkyl, optionally substituted C6-C10 aryl, optionally substituted C6-C10 alkylenearyl and optionally substituted C5-C10heteroaryl; R2 is selected from —H and optionally substituted C1-C6 alkyl; each of R3 and R4, independently of each other, is selected from —H, optionally substituted C1-C6 alkyl, optionally substituted C6-C10 aryl and optionally substituted C5-C10 heteroaryl; n is 0, 1, 2, 3 or 4. The derivatives have been prepared and their anticonvulsant profile was evaluated for the control of epileptic seizures.
US20080318939 Methods for treating ophthalmic disorders The invention relates in part to methods for treating ophthalmic conditions using compounds described herein. The conditions to be treated include various ocular cancers. The compositions employed include a polycyclic quinolinone derivative or related heteroaromatic analog thereof.
CN103120677A Application of Aphanamixoid A in medicine for treating or preventing renal fibrosis The invention provides an application of Aphanamixoid A in preparing a medicine for treating or preventing renal fibrosis, and belongs to the technical field fibrotic new application fibrotic the medicine. The application of the Aphanamixoid A in preparation of the medicine for treating or preventing the renal fibrosis is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on the renal fibrosis is inconceivably high; and the Aphanamixoid A has outstanding substantiality characteristic without possibility fibrotic any inspiration given by other compounds and obviously achieves the outstanding progress by being used for preventing and treating the renal fibrosis.
US8258305 Dopamine transporter inhibitors for use in treatment of movement disorders and other CNS indications The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.
CN1608617A Application of levocarnitine and its derivative in preventing and treating high altitude diseases The present invention relates to new medicinal application of levocarnitine as one kind of known compound and its derivative. Levocarnitine or its derivative is used as active component combined with one or several excipients and prepared via conventional process into tablet, capsule, oral liquid, injection, etc. for preventing and assisting treatment of high altitude diseases. The present invention is superior to available hormone medicine and diuretic medicine, which result in side effects, and hyperbaric oxygen therapy, which is inconvenient and has relatively low safety.
CN103356586A Application of Sarcaboside B in medicine used for treating rheumatoid arthritis Sarcaboside B capable of treating immunity inflammation is used for preparing a medicine used for treating rheumatoid arthritis, terfenadine and diclofenac sodium are taken as contrast, and Sarcaboside B has a definite curative effect. The invention discloses an application of Sarcaboside B in the medicine used for treating rheumatoid arthritis for the first time, a brand new skeleton type is adopted, and Sarcaboside B has unexpected rheumatoid arthritis treatment activity, no probability that any revelation is given by other compounds, outstanding substantial characteristic and an obvious progress when being used for treating rheumatoid arthritis.
CN1579417A Compound dewatered diuretic medicinal composition and its preparation method The invention discloses a compound desiccation and diuresis medicine compound and its manufacturing method, its ingredients have better effect within flowing weight shares: mannitol 100-200 shares, 1, 6-diphosphonic acid fructose 20-80 shares, sodium chloride 4-14 shares, the injection water is 1000 shares. The product can provide medicine quickly and the period is long, and it can reduce the side effect.
EP1531819A1 USE OF I kappa B KINASE INHIBITORS FOR THE TREATMENT OF PAIN The invention relates to the use of IκB kinase inhibitors that are suitable for producing medicaments for the treatment of pain. Suitable inhibitors are produced from compounds of formulas (I) and (Ia).
US20110319356 Methods Of Treating Optic Disorders The present invention relates to methods for treating optic disorders or for reducing or alleviating the signs, symptoms, or pathological conditions related to such optic disorders. In particular, methods are provided for treating optic disorders, or reducing the symptoms thereof, the methods involving the administration of one or more downstream folate compounds and/or methyl-B12. In one particular embodiment, the method comprises administration of L-methylfolate. In other embodiments, the method involves administering both L-methylfolate and methyl-B12. In still further embodiments, the method further involves reducing dietary intake of folic acid. In certain embodiments, the method further involves identifying a subject organism with a malfunction in one or more of the folate or B4 cycles. In certain embodiments, such a malfunction is one or more of the C677T and A1298C mutations. In still further embodiments, the method further involves identifying a subject organism that is deficient in vitamins B-12 and D3 but which possesses excess homocysteine.
EP2395968A1 Pharmaceutical composition comprising glucopyranosyl diphenylmethane derivatives, pharmaceutical dosage form thereof, process for their preparation and uses thereof for improved glycemic control in a patient The present invention relates to pharmaceutical compositions comprising a SGLT-2 inhibitor, pharmaceutical dosage forms, their preparation, their use and methods for treating metabolic disorders.
WO2009112674A3 Compounds for use in the treatment of neuropathic pain The present invention relates to the use of a beta-adrenergic receptor agonist as active ingredient for the production of a medicament for use in the treatment of neuropathic pain, in particular neuropathic allodynia, in particular chronic neuropathic allodynia, and more generally for the production of medicaments for relieving pain. The principal field of application of the present invention is the biomedical field, and more specifically the therapeutics field. The present invention aims in particular to provide a medicament which can be used as a substitute for the antidepressants currently used to treat pain. It finds a use in the human and veterinary clinical field.
US20100125071 Cxc-chemokine receptor ligands The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.
US7223857 Chain-shortened polynucleotide and method for preparation thereof The present invention provides a chain-shortened polynucleotide wherein the proportion of a 2′-5′ phosphodiester bond is up to 3% based on the whole phosphodiester bonds or a salt thereof and a pharmaceutical composition containing the same, and a method for producing the same.
CN101002734A Preparation of superfine powder containing anerthol trithione A superfine powder (1-20 microns) of anethol trithione is disclosed, which has high external stripping rate and biologic utilization rate.
WO2012034526A1 Fused heteroaryls and their uses Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.
US7943624 Pyridinylpyrazolopyrimidinone derivatives as PDE 7 inhibitors To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyridinylpyrazolo-pyrimidinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl or cycloheptyl group, R2 is methyl; R3 is a group: —NR5R6 or —S(O)0-2R8;hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; and R4 is methoxy or ethoxy group.
CN101953793A Preparation method of fructose diphosphate sodium powder injection The invention discloses a preparation method of a fructose diphosphate sodium powder injection, comprising the following steps of: decoloring, degerming, roughly filtering and finely filtering a fructose diphosphate sodium water solution; and punching, separating and crystallizing with ethanol or acetone and filling to obtain the aseptic powder injection. The fructose diphosphate sodium powder injection prepared by the method has higher purity, fewer impurities and more stable quality compared with the traditional products and is convenient to store and transport. The invention is simple to operate, has mild process condition and low cost and is suitable for industrial production.
CN102824317A New formulation containing bulleyaconitine A The invention relates to a new formulation containing bulleyaconitine A, relates to the field of medicines, and in particular relates to a new formulation which has pain-easing and anti-inflammation functions. The new formulation containing bulleyaconitine A is characterized by comprising the steps of: uniformly mixing bulleyaconitine A and auxiliary material, adding a wetting agent, manufacturing into a soft material and then into pellet, drying, and enteric coating so as to obtain the new formulation. Experiments show that the bulleyaconitine A is absorbed rapidly by a rat which is subjected to duodenal administration, cmanotherx can achieve 2.53ng/ml after 10min, which indicates that the bulleyaconitine A can be absorbed by small intestine, particularly the upper section of the small intestine. The absolute bioavailability of the duodenum group is 26.97+/-9.05% which is 1.8 times of the gavage medication administration group (15.36+/-3.47%), and therefore the intestinal solvent formulation of the bulleyaconitine A has higher curative effect than the common formulation.
CN1634062A Nose cavity administering formulation of nalmefene The invention provides a nalmefene preparation to be administered through nasal cavity, which comprises nalmefene, namefene free alkali or other pharmaceutically acceptable medicinal salt of nalmefene and absorption promoting agent, a large number of tests have shown that, the nasal cavity administered medicinal preparation by the invention can make the medicament absorbed through the path of nasal mucosa, and enter into blood circulation for actions. The advantages of the preparation include stabilized performance, controlled quality and non-stimulation to nasal cavity.
US20110028469 Thiphene-2-Carboxamide Derivatives As Modulators of CCR9 Receptor Provided are compounds of Formula (I) or of Formula (II) that are modulators of CCR9 receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or amelioratin diseases associated with modulation of CCR9 receptor activity.
US20110196035 Temporally-Controlled Treatment of Joint Disease A composition and method for treatment of osteoarthritis is disclosed. The composition includes at least one soluble injectable biocompatible carrier having a viscosity within prescribed limits and an amount of a calcium-channel blocker chosen in relation to the viscosity of the carrier. The concentration of the calcium-channel blocker in the joint synovial fluid is controlled according to the invention whereby effective treatment of osteoarthritis is provided.
US20110176994 Buoyant Polymer Particles for Delivery of Therapeutic Agents to the Central Nervous System The invention provides compositions and methods for treating a subject who has suffered from a central nervous system disorder. More particularly, the invention provides sustained polymeric drug delivery systems for direct delivery of therapeutic agents into the central nervous system.
US20080145457 Administering saponins to an animal The present invention relates to methods and compositions for reducing L-pipecolic acid concentrations and/or effects in animals. In an embodiment, the invention includes a method of reducing plasma concentrations of L-pipecolic acid in animals including administering an effective amount of a composition including saponins. In an embodiment, the invention includes a method of reducing anorectic effects of L-pipecolic acid in animals including administering an effective amount of a composition including saponins. Other embodiments are also included herein.
US20080318971 using bosutinib The present invention provides 4-anilino-3-quinolinecarbonitriles compounds useful for treating a subject having an BcrAbl positive leukemia that is resistant to imatinib.
CN102935088A Injection therapy and drug constitutes for curing recurrent aphthous ulcer The invention discloses injection therapy and drug constitutes for curing recurrent aphthous ulcer. Drug constitutes mainly comprise transfer factors, dexamethasone, mecobalamine and levoupivacaine. Drug constitutes are capable of improving local tissue nutrition and metabolism, improving local tissue cellular immunity, resisting inflammation, improving local symptoms and the like. The therapy has the advantages that the curative effect is high, materials can be obtained conveniently, the price is low and the operation is simple. A drug is injected for three times every week, and one course of treatment comprises six times of injection. The effective rate of the injection therapy is proved through clinical verification to exceed 98.5%.
US20080114003 Pyrimidinylisoxazole Derivatives The invention discloses isoxazole derivatives represented by a formula, in which R1 stands for hydrogen, lower alkyl, amino, halogen, lower alkoxy and the like, R2 stands for substituted or unsubstituted aryl and the like, R3 stands for hydrogen or lower alkyl, R4 stands for substituted or unsubstituted phenyl and the like, and Y stands for —CH2—, —CO—, —CH(CH3)—, —O—, —NH— and the like, or pharmaceutically acceptable salts thereof, which have excellent p38MAPkinase inhibitory action.
CN101264102A Alkaline sxidative externally-applied medicaments for treating skin disease The invention discloses an externally applied drug treating skin disease, in particular to an alkaline and oxidizing drug treating skin disease. The drug is characterized in that: a. For prescription 1, weight percentage of prescription is boric acid 15% to 20%, potassium nitrate 20% to 30%, sodium hydroxide 9% to 14%, ethanol 2% to 5% and the rest is purified water; pH value is 8 to 12, for prescription 2, boric acid 15% to 20%, benzoyl peroxide 5% to 10%, sodium hydroxide 9% to 16.5%, ethanol 2% to 5% and the rest is purified water; pH value is 8 to 12, pH value of medication for children is 9; b. The preparation process comprises the following: firstly boric acid and sodium hydroxide are added into purified water before stirred for dissolving to produce transparent solution; secondly, potassium nitrate or benzoyl peroxide is respectively added into the former solution, thirdly the rest sodium hydroxide is added for stirring and dissolving, finally ethanol is added for testing pH value. The alkaline and oxidizing drug treating skin disease has the advantages that: two kinds of water agent alkaline and oxidizing drug treating skin disease can popularly treat eczema, psoriasis, skin disease, skin itch, moisture, bromhidrosis, acne and ulcerate sore and furuncle; the drug can relieve pain of patient; population with osmidrosis disease cannot be affected in study, work and social intercourse; patient of each community can afford the drug with cheap price.
US7741325 Benzo[b]chromeno-naphthyridin-7-one and pyrano[2′,3′:7,8]quino[2,3-b]quinoxalin-7-one compounds A compound selected from those of formula (I): wherein: B1, B2 represent carbon or nitrogen, X, Y, X1 and Y1 represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, trihaloalkyl and NRaRb wherein Ra and Rb are as defined in the description, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, alkyl, —OR″a, —NR′aR′b, —O-Ta-OR″a, —NR″a-Ta-NR′aR′b, NR″a—C(O)-TaH, —O—C(O)-TaH, —O-Ta-NRa′Rb′, —NR″a-Ta-OR″a, —NR″a-Ta-CO2R″a and —NR″a—C(O)-Ta-NR′aR′b wherein R′a, R′b, R″a and Ta are as defined in the description, R3, R4 represent hydrogen or alkyl, A represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH—, —C(O)—CH(R8)— or —CH(R8)—C(O)— wherein R5, R6, R7 and R8 are as defined in the description, its isomers, N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.
CN101766622A Application of Morphine as medicament for protecting PC12 cells from injuries of Parkinson disease toxic substance The invention relates to an application of Morphine as a medicament for protecting PC12 cells from injuries of a Parkinson disease toxic substance, in particular to a new medical application of Morphine, belonging to the technical field of medicines. Through a thiazolyl blue (MTT) method, the Morphine is found to be capable of promoting the growth of adrenal gland chromaffin tumor cells (PC12 cells) of rats. The Morphine has the activity of promoting the proliferation of nerve cells and can inhibit nerve cell injuries caused by a Parkinson toxic substance MPP+(1-Methyl-4-Phenylpyridiniumion). Proved by a protein immunoblotting method, the Morphine can induce the expression level of thioredoxin in the PC12 cells, thus the Morphine for protecting the nerve cells from injuries of MPP+ toxicity is related to the induction of the expression of the thioredoxin.
WO2006041404A1 Substituted amino-compounds and uses thereof This invention relates to novel compounds having the structural formula Ia or formula Ib: Ia Ib and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
CN101182332B Manganese complexes having antitumor and affecting mitochondria functions and its preparation method The present invention provides a manganese complex with the anti-tumor function and the function of influencing mitochondria. A structural formula of the manganese complex is that N-allyl bipyridine methyl amine and MnCl2 are dissolved in methanol solution by the mol ratio of 1 to 1, and the temperature is controlled between 30 DEG C and 100 DEG C; the best reaction temperature is 80 DEG C, the reaction time is 2 to 8 hours, the best reaction time is four hours; the light yellow manganese complex is obtained after the methanol is removed. The manganese complex of the present invention has strong inhibition function towards tumor cells A549, Hela, HepG-2 and Eca109 and can induce the apoptosis of the tumor cells; the complex resist the mitochondria swelling function caused by Ca<2plus> by the dosage manner.
WO2013064620A1 18-methyl-6,7-methylene-3-oxo-17-pregn-4-ene-21,17β-carbolactones, pharmaceutical preparations comprising said compounds and use thereof in the treatment of endometriosis The present invention relates to 18-methyl-6,7-methylene-17-pregn-4-ene-21,17β-carbolactones of the general formula (I) where the 6,7-methylene group may be in the α or β position, to pharmaceutical preparations comprising at least one isomer of the formula (I) and to the use thereof in the treatment of endometriosis.
CN103536548A Oryzanol freeze-dried powder composition for injection, and preparation method thereof The invention provides an oryzanol freeze-dried powder composition for injection, and a preparation method thereof, and belongs to the field of medicine and medicine preparation technology. The main medicine ingredient of the oryzanol freeze-dried powder composition comprises, by mass, 0.1 to 99.9% of oryzanol, and 99.9 to 0.1% of chitosan nanoparticle. Beneficial effects of the oryzanol freeze-dried powder composition are that: 1) solubility of oryzanol in water is increased, and dissolving time is shortened, so that it is beneficial for clinical application; 2) antibacterial effect of oryzanol is increased, dosage of oryzanol in clinic can be reduced, and adverse reaction of oryzanol is reduced; 3) liquid is convenient for processing, and sterile operation processes are simplified; 4) chitosan is capable of encapsulating DNA effectively, protecting DNA from degradation, increasing lipid membrane fluidity, reducing membrane microviscosity, and changing membrane protein conformation, so that chitosan is beneficial for transmembrane transport of medicines; and 5) stability of the oryzanol freeze-dried powder composition is increased.
WO2008090717A1 Adam inhibitor Disclosed is an ADAM inhibitor which enables to prevent or improve conditions caused by increase in ADAM activity. Specifically disclosed is an ascorbic acid derivative represented by the general formula (1) below or a salt thereof. [chemical formula 1] (1) (In the formula, R represents a linear or branched alkyl group having 1-22 carbon atoms.)
CN1913879B Compositions and pharmaceutical uses for treating diabetes The subject invention provides compositions and methods for treating diabetes in patients. In a preferred embodiment, the invention provides compositions methods for treating diabetes and/or preventing or alleviating complications associated with diabetes. Specifically exemplified herein is the concurrent administration of a cysteamine compound with at least one additional therapeutic agent to prevent and/or treat diabetes as well as prevent and/or treat complications associated with diabetes. In a preferred embodiment, oral administration of cysteamine hydrochloride with Metformin to a patient diagnosed with diabetes can substantially regulate the patient's glucose metabolism and insulin sensitivity.
US20050271717 Dry-granulated dosage forms of tablets or capsules; preparation by compressing the mixture, milling, grinding or sieving the compressed material; hypercholesterolemia, hyperlipidemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's disease A unit dosage form comprising atorvastatin or a pharmaceutically acceptable salt thereof, prepared without a granulation step, wherein the measured atorvastatin potency of said dosage form shows a relative standard deviation (RSD) for atorvastatin potency per unit dosage form of not more than about 7.8%, when said unit dosage form is prepared at a rate that greater than 10,000 unit dosage forms per hour per single unit dosage form per machine, as well as the unit dsoage form in combination with at least one active drug, methods for preparing unit dosage form, kits for containing such compositions and a method of treating hypercholesterolemia and/or hyperlipidemia, osteoporosis, benign prostatic hyperplasia (BPH), and Alzheimer's Disease using a therapeutically effective amount of the unit dosage form.
US7074769 Antisense oligonucleotide or analog thereof comprising 10 or more contiguous bases or base analogs; for treating cancer This invention provides an antisense oligonucleotide or analog thereof comprising 10 or more contiguous bases or base analogs from the sequence of bases of sequence A, B, C, D, E, F, G, H, I, J, K, L, or M of FIG. 1. This invention also provides the above-described antisense oligonucleotides, wherein the nucleotide sequence comprises nucleotide sequence A, A′, B, C, C′, D, E, E, E′, F, G, G′, H, H′, I, I′, J, K, K′, L, L′, M, or M′ of FIGS. 2A and 2B. This invention also provides the above-described antisense oligonucleotides, wherein the oligonucleotide is encapsulated in a liposome or nanoparticle. This invention also provides the above-described antisense oligonucleotides, wherein the phosphate backbone comprises phosphorothioate bonds. In addition, this invention provides a method of treating cancer, comprising introducing into a tumor cell an effective amount of the the above-described antisense oligonucleotide, thereby reducing the levels of bcl-xL protein produced and treating cancer. This invention also provides the above-described methods, wherein the introducing comprises using porphyrin or lipofectin as a delivery agent. This invention also provides the above-described pharmaceutical compositions, wherein the oligonucleotide is encapsulated in a liposome or nanoparticle. This invention further provides the above-described pharmaceutical compositions, wherein the pharmaceutical composition comprises tetra meso-(4-methylpyridyl)porphine or tetra meso-(anilinium)porphine or a combination thereof.
WO2012015487A1 Combination of dapsone with adapalene A composition suitable for topical application that contains at least two active ingredients, one of these being dapsone and one selected from the group consisting of adapalene, tazarotene and treinion for the effective treatment of acne and other dermatological conditions.
EP1659970A1 Sytem and method for prevention of radiocontrast induced nephropathy An apparatus and method particularly useful in treatments and therapies directed at the kidneys such as the prevention of radiocontrast nephropathy (RCN) arising from diagnostic procedures using iodinated contrast materials. A series of treatment schemes are provided based upon local therapeutic agent delivery to the kidneys that can be used as a prophylactic treatment for patients undergoing interventional procedures that have been identified as being at an elevated risk for developing RCN as well as for low risk patients. The methods may include pre-exposure and post contrast exposure treatments alone or in combination with the local delivery of therapeutic agents to the kidneys. Among the agents identified for such treatments are normal saline and the vasodilators papaverine and fenoldopam mesylate and appropriate dosing is provided.
WO2008106168A1 Combination of imidazo [1,5-a] pyrazinyl derivatives with an agent that inhibits serine phosphorylation of irs1 for use in the treatment of cancer Compositions and methods for treating tumors or tumor metastases in a patient, comprising administering to a patient simultaneously or sequentially a therapeutically effective amount of an agent which inhibits serine phosphorylation of IRS1 and an IGF1 R inhibitor compound of Formula I, such as c/s-3-[8-Amino-1-(2-phenyl-quinolin-7-yl)-imidazo[1,5- a]pyrazin-3-yl]-1-methyl-cyclobutanol, or a pharmaceutically acceptable salt thereof.
WO2014017999A1 Method for producing an agent for the treatment of tuberculosis The preparation for the treatment of tuberculosis relates to the chemical and pharmaceutical industry and to medicine. The preparation for the treatment of tuberculosis, which contains isoniazid as the active substance and water for injection as an auxiliary component, according to the invention additionally contains, as auxiliary components, methionine, succinic acid, and sodium succinate. The novel composition of the preparation makes it possible to increase the storage temperature of said preparation, which is important in the transportation and storage thereof, and also to decrease the toxicity of the effect thereof on the body during tuberculosis treatment.
WO2009045337A1 Chemical sterilant for adult male dog population control, comprising a mineral gluconate and an amino acid A chemical composition for use in controlling the population of free-roaming, sexually mature male dogs. The chemical sterilant is injected in a manner that the dog's appearance and secondary male sexual characteristics are preserved such that the dog maintains its position in the hierarchy of the free-roaming dogs while not contributing to the number of puppies produced. A reduction in the number of free-roaming dogs reduces the number of human victims of dog-bite acquired rabies. Because the appearance and nature of the sterilized dog is substantially unchanged, the chemical composition is acceptable to the human community that the dog habitats.
US20110269790 Novel thienopyridines as pharmacologically active agents The present invention provides compounds and pharmaceutically acceptable salts thereof methods for synthesizing thienopyridines and methods for inhibiting TNF-α activity for the treatment of cancer, asthma, arthritis, diabetes and inflammation. Provided are compounds of formula (I).
WO2014069792A1 Pack for supplying carbon dioxide to skin The present invention provides a pack for supplying carbon dioxide to the skin, which can be used as a pack for allowing carbon dioxide to act on the skin, does not undergo deterioration in quality thereof even when preserved for a long period, is easy to use, and has a simple constitution. In the pack, a non-woven fabric having an acid coating layer formed on one surface thereof and a non-woven fabric having a carbonate salt coating layer formed on one surface thereof are laminated and bonded to each other in an integral manner so that the acid coating layer and the carbonate salt coating layer can face each other, and water-proof paper is attached onto one outer surface of the pack.
CN103263406A Use of DHA, epa or DHA-derived EPA for treating a pathology associated with cellular oxidative damage The invention relates to medicine rich in docosahexaenoic acid (DHA)or eicosapentaenoic acid (EPA) or DHA-derived EPA for treating a pathology associated with cellular oxidative damage, more specifically, the medicine is used for the treatment of ,eurodegenerative diseases,oculopathy,ischemic disease, inflammatory disease,atherosclerosis, disease associated with DNA oxidative damage and disease associated with physical exercise.
CN101210009A Bruguiesulfurol, derivatives and preparation method thereof, and application for the same in preparing diabetes treatment medicament The invention relates to the field of pharmaceutical technology, in particular to a compound-new bruguiesulfurol separated from a mangrove plant, bruguiera gymnorrhiza, ramification thereof, a preparation method thereof and application thereof on preparing medication used for treating II type diabetes. The constitutional formula of the new bruguiesulfurol and the ramification thereof is showed in the formula, when R is hydrogen, namely, is the new bruguiesulfurol. The compound and the ramification thereof passes through biological activity assay and can be employed as protein-tyrosine-phosphatase 1B (PTP1B) inhibitor and insulin sensitizer, which can be used for preparing the medicines for treating II-type diabetes, adiposity and other complications caused by diabetes and adiposity.
WO2011030312A1 NOVEL INHIBITORS OF STEAROYL-CoA-DESATURASE-1 AND THEIR USES The present invention relates to inhibitor of the activity of stearoyl-CoA-desaturase-1 (SCD-1) enzyme for use in the treatment of prostate cancer as well as to novel inhibitors of formula (IIa):
CN103349669A Malic acid-containing composite dialysis preparation and preparation method thereof The invention discloses a malic acid-containing composite dialysis preparation and a preparation method thereof. The composite dialysis preparation comprises an agent A and an agent B, wherein raw materials of the agent A comprise, by weight, 10-30 parts of sodium chloride, 0-2 parts of potassium chloride, 0.5-2 parts of calcium chloride, 0.2-0.5 part of magnesium chloride, 0.1-8 parts of malic acid, 0-8 parts of malate, 0-5 parts of glucose, and 0-8 parts of a pH value buffering agent, and a raw material of the agent B comprises, by weight, 5-10 parts of sodium bicarbonate. With the present invention, special treatment effects are provided in the fields of cellular immunity improvement, myocardial coordination improvement, tumor necrosis factor reduction, serum phosphorus content reduction, CO2CP increase, dialysis imbalance disorder treatment and the like.
CN102579528A Medicine composition for preventing and curing prostatic diseases The invention discloses a Centella asiatica (L.) Urban medicinal composition for preventing and curing diseases of prostatitis, prostatic hyperplasia and the like. The composition is obtained by extracting from dry herbs or rooted herbs of Centella asiatica (L.) Urban and purifying. The composition is characterized in that the composition comprises asiaticosides, madecassosides, asiaticoside B, quercetin, kaempferol and the like. Pharmacological tests of the composition prove that the composition has the effects of the prevention and the curing of prostatitis, prostatic hyperplasia and the like. The composition has a new use in the preparation of medicines for preventing and curing prostatic diseases. The invention also discloses a medicinal preparation of the composition, which can be anyone of a tablet, a capsule, a pill, a granule, a suspension, a dropping pill, an ointment and a suppository rectal administration preparation.
WO2009065846A1 A method for treating addiction A method for treating addiction, in particular nicotine addiction, alcohol addiction and drug addiction, such as opioid addiction. The invention furthermore relates to novel pharmaceutical compositions for the treatment of addiction comprising a therapeutically effective amount of a compound of formula (I).
EP1377560B1 Piperazine derivatives as tachykinin antagonists The present invention relates to piperazine derivatives of formula (I) wherein R and R1 represent independently halogen or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; n and m are independently 1 or 2 and pharmaceutically acceptable salts and solvates thereof, to process for their preparation, to pharmaceutical compositions containing them and to their medical use.
CN101597212A Kirenol derivative and application thereof in preparation of proinflammatory cytokine inhibitor The invention relates to a Kirenol derivative and an application thereof in preparation of a proinflammatory cytokine inhibitor. The Kirenol derivative shown in a general formula (I) and a general formula (II) can inhibit the proinflammatory cytokine tumor necrosis factor (TNF)-alpha, the interleukin (IL)-1beta and the inflammatory molecule nitrogen oxide and is suitable for drug preparation.
CN103251643A Application of Polyflavanostilbene A in preparing anti-lung cancer metastasis medicine The invention discloses an application of Polyflavanostilbene A in preparing an anti-lung cancer metastasis medicine, belonging to the technical field of a new application of a medicine. The Polyflavanostilbene A can inhibit the movement and transfer abilities of tumor cells. The application of the Polyflavanostilbene A in preparing an anti-lung cancer metastasis medicine, disclosed by the invention, is disclosed for the first time, the framework type is a brand new framework type, and the metastasis inhibition activity of the Polyflavanostilbene A on lung cancer cells is unexpectedly strong.
CN1802958A Method for preparing stomach-benefiting, digestion-promoting milk comprising micron pine pollen, fig, chickens gizzard-membrane etc. The invention relates to a process for preparing stomach-benefiting and spleen-enlivening milk liquid, which is prepared from various conventional milks and air flow super fine disintegrated micrometer pine pollen powder, micrometer bee pollen, micrometer bee pollen, micron haw powder, micrometer chicken's gizzard-skin powder, micrometer hericium erinaceum powder, micrometer radish seed powder and oligosaccharide as raw materials through combination. The invention achieves the functions of digestion-promoting, spleen-enlivening, fatigue-resisting, and human body immunity-improving.
CN101954084A Medicinal composition for treating mixed infection in livestock and poultry and preparation method thereof The invention relates to a medicinal composition for treating mixed infection in livestock and poultry and a preparation method thereof, and belongs to the technical field of veterinary preparations. The medicinal composition comprises sulfamethoxydiazine sodium, enrofloxacin and a non-steroidal analgesic-antipyretic medicament, is a liquid preparation for injection, treats the mixed infection in livestock and poultry and also can effectively relieve fever and other clinical symptoms so as to achieve the effect of treating both principal and secondary aspect of disease. Compared with a single medicament, the compound medicinal composition has the advantages of obviously improving the clinical curative effect, reducing stress response of ill animals, and contributing to body rehabilitation so as to provide a high-efficiency medicament for treating the mixed infection in livestock and poultry for clinical veterinarian. The invention also provides a method for preparing the medicinal composition.
WO2010007629A1 A kit comprising anti-emetic and oral contraceptive A kit for administration of emergency contraception comprising an oral contraceptive and an antiemetic, administered simultaneously or sequentially. A pharmaceutical combination comprising separate dosage forms, in a common package, of oral contraceptive and an anti-emetic useful in reducing nausea and vomiting associated with the administration of oral contraceptive. A kit for administration of emergency contraception comprising an oral contraceptive and an antiemetic wherein the antiemetic in immediate release formulation is administered prior to the administration of oral contraceptive.
US20110086878 Treatments for Neuropathy Small fiber neuropathy is treated or prevented by topically administering to a subject in need thereof topically active quinoline compounds or pharmaceutically acceptable salts thereof under conditions effective to treat or prevent neuropathy in the subject. Glial cell-derived neurotrophic factor (GDNF) receptors are modulated with the subject active quinoline compounds, which may be formulated in topical lotions.
US8399436 N-pyrazolyl carboxamides as CRAC channel inhibitors The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.
EP2465358A1 Method for manufacturing a functional gel At first fill the airtight container 2 with water (solution), and supply a gas such as hydrogen from the gas supply pipe 5, drive the supersonic wave vibratory plate 4, then the micro-bubbles 1b of the gas are generated. The diameter of the micro-bubbles 1b is for example nanosize, then the speed of rise in the water is slow, so it remains underwater for about 10 minutes even if the supersonic wave vibratory plate 6 is stopped.
EP1954678A1 Novel nk1 and nk2 antagonists The present invention relates to novel 3-cyano-naphthalene-1-carboxylic acid perhydroxyalkylmethyl-piperazine compounds of formula I which are antagonistic to tachykinin receptors. The present invention is further directed to pharmaceutical compositions comprising such compounds, to processes for the preparation of such compounds and to intermediate products of these processes.
WO2013147689A1 Combination treatment comprising sulphated glycosaminoglycans for inducing labor The present invention refers to the use of certain sulfated glycosaminoglycans for inducing labor. The sulfated glycosaminoglycans have a reduced anticoagulant activity and are used in a combination therapy together with treatment capable of promoting cervical ripening or capable of promoting myometrial contractions of the uterus.
CN1695740B Composite body of fiber protein adhesive and antibiotics in use for treating infection in deep part, and application A fibrin gel-antibiotic compound for treating deep infection by local application is disclosed. Said antibiotic chosen from gentamycin and butylamine cristalomicine is contained proportionally in the fibrin gel as the slowly-releasing carrier.
CN101817746A Phenolic acid compound and use thereof in the preparation of anticomplementary medicaments The invention relates to a phenolic acid compound and use thereof in the preparation of anticomplementary medicaments. The phenolic acid compound has a chemical structure formula shown in the specification; when R1 is COOH, and R2 is OCH3, the compound is vanillic acid; and when R1 is-CH=CH-COOH, and R2 is H, the compound is para-hydroxycinnamic acid. The invention has the advantages that the phenolic acid compound is directly extracted from natural product, and the compounds of vanillic acid and para-hydroxycinnamic acid have better inhibition function to the classical pathway of a complement system.
CN101250181A S-pantoprazole sodium The invention relates to S-pantoprazole sodium, a relative preparation method and an application. The S-pantoprazole sodium is characterized in that its chemical approved name is (S)-5-difluoromethoxy-2-[(3, 4-dimethoxy-2-pyridyl) methyl] sulfinyl-1H-sodium benzimidazole in amorphous solid type, whose water content is 0.1-1.9%. The preparation method comprises (a) mixing S-pantoprazole and tetrahydrofuran, adding sodium hydride and reacting, wherein the mol ratio between the sodium hydride and S-pantoprazole is 1:1, and the volume of the added tetrahydrofuran is 2-50 times of the mass of S-pantoprazole, (b) adding ether into the reaction liquor to crystallize S-pantoprazole sodium, wherein the added amount of ether is 1-10 times of the volume of tetrahydrofuran, (c) filtering the crystallization liquid and drying in vacuum to obtain amorphous S-pantoprazole sodium, wherein the drying temperature is 20-50DEG C.
US20090239943 Nutraceutical composition and methods for its use A composition for inhibiting the activity of NF kappa B or for inhibiting tissue damage inflammation due to disease including a combination of green tea polyphenols; resveratrol; soy isoflavones, and curcumin. Also disclosed is a method of inhibiting the activity at the NF kappa B or inflammation using the composition.
CN101375947A Compound Macleaya cordata injection and preparation method The invention discloses a compound macleaya cordata injection applied to treating piglet's yellow-white dysentery and a preparation method. The macleaya cordata injection is composed of 20-100 parts of macleaya cordata, 10-50 parts of sulphuric acid berberine, 30-100 parts of enrofloxacin, 1-20 parts of sulphuric acid atropine, 5-50 parts of trimethoprim and 200-400 parts of propylene glycol. The preparation method comprises the steps of weighing the constituents according to weight; heating the propylene glycol to 75-85 DEG C, adding the trimethoprim to be stirred and dissolved; taking water for injecting with a proper volume, orderly adding the macleaya cordata, the sulphuric acid berberine and the sulphuric acid atropine to be stirred and dissolved; taking water for injecting with a proper volume, orderly adding sodium hydroxide and enrofloxacin to be stirred and dissolved; combining the prepared solutions to be stirred evenly, keeping for 15-20 min, adding water for injecting to 1000 parts after the liquid medicine is clarified. The invention adopting the compound preparation has the advantages of quick effect, low residue, no recurrence and the like, improves livability of pigs, and increases weight of pigs.
US20080027009 Surfactant Preparation Having Reduced Enzyme Damaging A method of protecting skin enzymes from the harmful effects of a cosmetic cleansing preparation which comprises water and one or more anionic surfactants. The method comprises using a cleansing preparation which has a pH value of from 4 to 7 and an SCTE (Stratum Comeum Tryptic Enzyme) value, determined following application of the preparation to human skin and standardized to a value of 100 for tap water, of from 65 to 95. The preparation comprises (i) one or more acyl-/dialkylethylenediamines which reduce the CMC of the one or more anionic surfactants and (ii) a buffer system of citric acid and citrate ions.
EP1202734B1 3(5)-ureido-pyrazole derivatives, process for their preparation and their use as antitumor agents 3-ureido-pyrazole derivatives represented by formula (I): where R, R1 and R2 are as described herein, or pharmaceutically acceptable salts thereof; are useful, for example, for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
CN1965859A Sodium selenite solution containing clustered water used for animal The invention relates to a method for using sodium selenate to prepare wide-spectrum antibiosis solution, wherein it uses hexacyclic ring water as carrier that adds frozen hexacyclic ring water into sodium selenate solution, to reduce the volume of hydrone group, the viscosity and surface tension, to reduce the expand resistance and accelerate the drug release. The hexacyclic ring water has strong affinity with cell, to improve the treatment effect on animal bacterial and mycoplasma affection.
CN102824360A Powder composition containing glucose and preparation method thereof The invention relates to a powder composition containing glucose and a preparation method thereof. Specifically, the powder composition comprises glucose, halogen salt of potassium, halogen salt of sodium and the like. The powder composition has excellent medical performance.
US20050154025 6-[4-(fluoro- or trifluoromethyl)pyridyl-4-(p-fluorophenyl)-5-methylimidazol-2-yl] pyridones; cyclization of 1-phenyl-1-pyridyl-1,2-diaminopropanes with an acid, amidine, or nitrile compound; neuropeptide Y receptor antagonists; cardiovascular and central nervous system disorders, metabolic diseases A compound of the formula (I): wherein R1 is hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy, lower alkoxy or aralkyloxy; R2 and R3 are each independently hydrogen, halogen or halo-lower alkyl; and R4 and R are each independently hydrogen or halogen, is useful as a pharmaceutical composition for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, etc., nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
CN101602728A N-substituted benzene ring 3,5-pyrazodione compounds, preparation method and application thereof The invention belongs to the technical field of chemical synthesis of medicaments, and discloses N-substituted benzene ring 3,5-pyrazodione compounds with antitumor activity, a synthesis method and application thereof. The compounds have a structure shown in a general formula I, wherein in the formula, R1 is hydrogen, m-methyl, p-methyl, p-chlorine, and p-bromine; R2 is p-benzyloxy, p-hydroxy, p-chlorine, and p-bromine; R3 is n-butyl, isobutyl, cyclopropyl methyl, and benzyl; and R4 is hydrogen or hydroxy. The compounds are used for treating tumor diseases; and in vitro anticancer activity experiments prove that the compounds have obvious inhibition and killing effects on a plurality of tumor cells, and can be taken as active components to be applied to clinical prevention and treatment of cancer after the compounds are developed into novel medicaments.
WO2007014198A1 1, 2, 3 -triazoles inhibitors of tubulin polymerization for the treatment of poliferative disorders The invention relates to compounds of structural formula (I): formula (I) or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
WO2013142205A1 Pharmaceutical compositions comprising benzyl alcohol The present invention relates to a pharmaceutical composition comprising benzyl alcohol and polyoxyethylene derivatives of sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.
EP0833622B1 Compositions comprising a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor Combinations of a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor are described for treatment of inflammation and inflammation-related disorders.
CN102204922A Solid preparation of sodium fosinopril and hydrochlorothiazide medicinal composition The invention discloses a liposome preparation of sodium fosinopril and hydrochlorothiazide. The liposome is mainly prepared from the following components in part by weight: 10 to 20 parts of sodium fosinopril, 12.5 parts of hydrochlorothiazide, 50 to 200 parts of soybean phosphatidylcholine, 20 to 100 parts of cholesterol and 5 to 60 parts of sodium deoxycholate. The invention also discloses a solid preparation of a sodium fosinopril and hydrochlorothiazide medicinal composition, which is prepared from the liposome preparation of sodium fosinopril and hydrochlorothiazide, and other excipients usually used pharmaceutically. The quality of the preparation is improved and the toxic and side effects are reduced.
US20080299226 Hemostatic Agent Composition and Method of Delivery A hemostatic agent composition that includes a clay hemostatic agent which is inert and non-reactive relative to blood clotting proteins and platelets, yet is capable of accelerating the formation of a stable clot when applied to an actively bleeding wound.
CN103656244A Partial nursing matter capable of improving discomfort after healing of knife cut wounds The invention discloses a partial nursing matter capable of improving the discomfort after the healing of knife cut wounds and aims to solve the treatment problem that the wounds feel uncomfortable after a suturing surgery. The partial nursing matter is characterized by being prepared from following crude drugs in parts by weight: blackend swallowwort root, Chinese buckeye seeds, loose knots, rice-paper plants, semen litchi, ivy glorybind herb roots, paris polyphylla, asterina pectinifera, aralia chinensis, mustard plaster powder, magnets and lobed kudzuvine roots. Clinical experiments show that the partial nursing matter has the characteristics of good curative effects and higher safety on treating the discomfort of the wounds after the suturing surgery. The partial nursing matter is worthy of being clinically applied and popularized.
EP1496903A1 Anhydrovinblastine for the treatment of cancer The use of a derivative of vinblastine, 3', 4'-anhydrovinblastine (AHVB), in the treatment of cancer in a mammal is provided. AHVB is found to be effective in the treatment of advanced and metastatic cancers. Effective dosages of between about 2 and about 30 mg/m2 are provided.
CN103169972A New application of statin compound as topical medicine for preventing and curing osteoporotic fracture The invention discloses a new application of statin compound as topical medicine for preventing and curing osteoporotic fracture and enhancing bone plant strength in osteoporotic bone, particularly, discloses a topical statin composite for bone. The topical statin composite can increase bone mass, improve bone density, improve bone tissue microstructure and enhance bone mechanical property, thereby being used for preventing and curing osteoporotic fracture and enhancing the bone plant strength in osteoporotic bone.
CN101569628B Cefmenoxime hydrochloride composition powder injection and manufacturing method thereof The invention relates to a cefmenoxime hydrochloride composition powder injection, which comprises the following components: 100-150 parts of cefmenoxime hydrochloride, 30-35 parts of natrium carbonicum calcinatum, preferably 125 parts of cefmenoxime hydrochloride and 33 parts of natrium carbonicum calcinatum. The grain size of the cefmenoxime hydrochloride is 400-600 meshes, which is preferably 500 meshes. The manufacturing method of the cefmenoxime hydrochloride composition powder injection comprises the steps as follows: 100-150 parts of cefmenoxime hydrochloride and 30-35 parts of natriumcarbonicum calcinatum are respectively sieved, evenly mixed and pulverized until the grain size of the cefmenoxime hydrochloride is 400-600 meshes and is preferably 500 meshes; the obtained powder issub-packaged into sterilized vials and is plugged. The cefmenoxime hydrochloride composition powder injection prepared by the invention has the advantages of fine quality, rapid dissolution and good stability after being prepared into solution.
US20100179114 S-Isomer of 2- piperidine and Other Dermal Anesthetic Agents The present invention relates to the S-isomers of anesthetic compounds, the methods of treatment therewith, the compounds being useful for inducing local anesthesia, analgesia and sleep.
WO2014144075A1 Anticholinergic glycopyrrolate esters for the treatment of hyperhidrosis Use of a compound having the formula (I) in the preparation of a medicament composition comprising from about 1.0% to about 25% of said compound and a pharmaceutically acceptable vehicle, for topical administration to skin of an area of a mammalian subject suffering from hyperhidrosis, before bedtime, such that compared to untreated, baseline conditions, sweat production is reduced by at least about 25% for at least about six (6) hours.
CA2218714C Dosage form comprising oxybutynin A composition comprising oxybutynin and a device comprising oxybutynin are disclosed for oxybutynin therapy.
WO2005012294A1 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
WO2006127368A2 Methods for synthesizing imidazotriazinones Methods of synthesizing imidazotriazinones, such as vardenafil, and compositions useful for the same are disclosed.
US20050123512 Binding agents, vectors, host cells; gene therapy; nucleotide sequence with DNA insert encoding polypeptide; genetic engineering; medical diagnosis The present invention provides novel Interleukin-1 Receptor Antagonist-Like (IL-1ra-L) polypeptides and nucleic acid molecules encoding the same. The invention also provides selective binding agents, vectors, host cells, and methods for producing IL-1ra-L polypeptides. The invention further provides pharmaceutical compositions and methods for the diagnosis, treatment, amelioration, and/or prevention of diseases, disorders, and conditions associated with IL-1ra-L polypeptides.
WO2014049356A1 Erythromycin ketolide derivatives bearing c-10 modifications The invention provides novel antibiotics, pharmaceutical compositions containing them and their medical use, for example in the treatment or prevention of microbial infections. Provided are compounds of Formula I, pharmaceutically acceptable salts and prodrugs thereof:
US20080051319 Inhibiting JNK Signaling Promotes CNS Axon Regeneration Regeneration of a lesioned CNS axon of mature neuron, determined to be subject to regeneration inhibition by endogenous cJun-N-terminal kinase (JNK), is promoted by contacting the neuron with an exogenous JNK inhibitor at a concentration sufficient to partially inhibit the JNK, and thereby promote a resultant regeneration of the axon.
WO2014070038A1 Solid dosage form having neuroprotective, antiamnesic, antioxidant, antihypoxic and anti-ischemic activity (variants) The invention relates to the pharmaceutical industry and the field of medicine and can be used in the creation and administration of solid dosage forms having neuroprotective, antiamnesic, antioxidant, antihypoxic and anti-ischemic activity. The aim of the present invention is to create a solid dosage form having neuroprotective, antiamnesic, antioxidant, antihypoxic and anti-ischemic activity, by means of using 2-ethyl-6-methyl-3-hydroxypyridine succinate, mineral substances, 13С isotopes and 15N isotopes. The technical results of the invention are a more rapid onset of therapeutic effect, an enhanced therapeutic effect with no increase in the concentration of the 2-ethyl-6-methyl-3-hydroxypyridine succinate preparation, and improved stability for the duration of the shelf life.
CN101928227A Mutual prodrug of 6-methoxyl-2-naphthylacetic acid and salicylanilide compounds, preparation method and application thereof The invention discloses a mutual prodrug of 6-methoxyl-2-naphthylacetic acid and salicylanilide compounds, which has the chemical structural formula shown in (I) or optical isomer (II). A preparation of the mutual prodrug of 6-methoxyl-2-naphthylacetic acid and salicylanilide compounds is characterized in that with 6-methoxyl-2-naphthylacetic acid and salicylanilide compounds as starting materials, esterification is carried out in an organic solvent for preparing the mutual prodrug. The mutual prodrug of the 6-methoxyl-2-naphthylacetic acid and salicylanilide compounds can be used for treating inflammation and analgesia as well as abatement of fever. Acute toxicity experiments prove that the prodrug is safe and low in toxicity.
WO2010056847A3 Lyophilization formulation This invention relates to a pharmaceutical kit containing a lyophilized preparation of a pyrimidine compound described in the specification. Also disclosed is a lyophilization process for making this preparation.
WO2006056427A1 Novel 4-arylamino pyridone derivatives as mek inhibitors for the treatment of hyperproliferative disorders The invention provides novel, substituted 4-arylamino pyridone compounds (formula (I)), pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R 1, R2, R9, R 10, R 11, R 12, R 13, R 14 and L are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
US20110021497 Amino triazoles as pi3k inhibitors The invention relates to compounds of formula (I) wherein X, T1 and R1 to R3 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
US20080167245 Novel metastasis suppressor gene on human chromosome 8 An isolated or purified nucleic acid molecule consisting essentially of a nucleotide sequence encoding the metastasis suppressor gene located at p21-p12 on chromosome 8 of a human (Tey 1), a variant Tey 1, or a fragment of either of the foregoing comprising at least 455 contiguous nucleotides; an isolated or purified nucleic acid molecule consisting essentially of a nucleotide sequence that is complementary to a nucleotide sequence encoding Tey 1, a variant Tey 1, or a fragment of either of the foregoing comprising at least 455 contiguous nucleotides; a vector comprising any of the foregoing, wherein, when the isolated or purifies nucleic acid molecule consists essentially of a nucleotide sequence encoding Tey 1 or a variant thereof, the isolated or purified nucleic acid molecule is optionally part of an encoded fusion protein; a cell comprising and expressing any of the foregoing isolated or purified nucleic acid molecules, optionally in the form of a vector; an isolated or purified polypeptide molecule consisting essentially of an amino acid sequence encoding Tey 1, a variant Tey 1, or at least 6 contiguous amino acids of either of the foregoing; a conjugate or a fusion protein comprising a therapeutically or prophylactically active agent, and an excipient or an adjuvant, a method of treating cancer prophylactically or therapeutically in a mammal comprising administering to the mammal an effective amount of (a) an isolated or purified nucleic acid molecule encoding Tey 1, optionally in the for of a vector, or (b) an isolated or purified Tey 1 polypeptide, optionally in the form of a conjugate or fusion protein, whereupon the mammal is treated for the cancer prophylactically or therapeutically; a method of diagnosing cancer comprising (a) obtaining a test sample from the mammal, and (b) assaying the test sample for the level of Tey 1, wherein a decrease in the level of Tey 1 in the test sample as compared to the level of Tey 1, wherein a decrease in the level of Tey 1 in the test sample as compared to the level of Tey 1 in a control sample is diagnostic for the cancer, and a method of prognosticating cancer in a mammal comprising (a) obtaining a test sample from the mammal, and (b) assaying the test sample for the level of Tey 1, wherein an increase in the level of Tey 1 over time is indicative of a positive prognosis and a decrease in the level of Tey 1 over time is indicative of a negative prognosis.
US20110111041 Bacterially derived intact minicells that encompass plasmid free functional nucleic acid for in vivo delivery to mammalian cells Intact, bacterially-derived minicells can safely introduce therapeutically effective amounts of plasmid-free functional nucleic acid to target mammalian cells. To this end, functional nucleic acid can be packaged into intact minicells directly, without resort to expression constructs, the expression machinery of the host cell, harsh chemicals or electroporation.
US20120129810 Combination antineoplastic therapy The present invention is directed to methods of using a sirolimus drug and chloroquine or a quinoline derivative in combination. Methods of use are also described.
CN103373966A 4-anilino quinazoline amido derivatives as well as preparation methods and applications thereof The invention discloses 4-anilino quinazoline amido derivatives. The 4-anilino quinazoline amido derivatives are characterized by having the general formula as described in the description, wherein R is one of the groups as described in the description, and X is Cl or B. Particularly, the X is Br if the R is one group, and the X is Cl if the R is another group. The 4-anilino quinazoline amido derivatives disclosed by the invention can be used for preparing anti-cancer medicaments. The invention further discloses the preparation methods of the 4-anilino quinazoline amido derivatives.
US7989182 Nucleic acid encoding SCN1A variant A method of identifying a subject predisposed to a disorder associated with ion channel dysfunction, comprising ascertaining whether at least one of the genes encoding ion channel subunits in said subject has undergone a mutation event such that a cDNA derived from said subject has the sequence set forth in one of SEQ ID NOS: 1-134.
CN102058609A Application of polydatin to preparing antineoplastic drug The invention belongs to the field of antineoplastic drug preparation and relates to novel application of polydatin to preparing the antineoplastic drugs. The invention also provides an antineoplastic drug, wherein the main active component of the antineoplastic drug is polydatin. In the invention, the proliferations of cells such as breast cancer, lung cancer, liver cancer, ovarian cancer, cervical cancer, nasopharyngeal cancer, leukemia and the like treated by the antineoplastic drug polydatin are all restrained obviously; a cell cycle analysis shows that the S phase in the cell cycle is retardant and cell apoptosis is induced; and the polydatin with low concentration has the effect of restraining the migration and the conglutination of a tumor cell. In the invention, while the antineoplastic drug polydatin increases the treatment effect of a malignant tumor and reduces the incidence rate of relapse and transfer of a tumor patient, the toxic and side effects are obviously reduced compared with the traditional clinical commonly used chemotherapeutic drugs, therefore, the lifetime of a malignant tumor patient is prolonged, and the life quality of the malignant tumor patient is improved.
US20110065696 Imidazoyl pyridine compounds and salts thereof A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, X1 represents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by Aβ.
US20090275644 Novel adaptor protein that binds to mammalian toll-like receptor 3 and gene thereof A novel adaptor protein and its gene are provided. The novel adaptor protein has a property of binding to mammalian Toll-like receptor 3, which controls type I interferon production that is effective for prevention/treatment of viral infectious disease such as hepatitis B, hepatitis C, and the like, treatment of tumors, and the other purposes. Novel adaptor protein TICAM-1, which has an amino acid sequence set forth in SEQ ID NO: 2 or 4, specifically binds to the mammalian Toll-like receptor 3 and induces production of type I interferon. A mutant of the adaptor protein TICAM-1 has similar properties, provided that it has TIR domain (an amino acid sequence ranging from 394-position to 532-position in the amino acid sequence set forth in SEQ ID NO: 2 or an amino acid sequence ranging 396-position to 534-position in the amino acid sequence set forth in SEQ ID NO: 4). The gene is a gene encoding the adaptor protein TICAM-1.
WO2009103007A3 Steroid hormone receptor modulator compounds and methods This invention relates to compounds that bind to intracellular receptors and/or modulate activity of intracellular receptors, and to methods for making and using such compounds.
WO2013170965A1 Pharmaceutical composition comprising (1r,4r)-6'-fluoro-n,n-dimethyl-4-phenyl-4',9'-dihydro-3'h-spiro[cyclohexane-1,1'-pyrano [3,4,b]indol]-4-amine and antidepressants The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1'-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is an antidepressant.
US7262164 Polymeric thiol-linked prodrugs employing benzyl elimination systems Thiol-linked polymeric prodrugs, methods of making and using the same are disclosed. The use of a sulfhydryl bond in combination with a benzyl elimination system results in the formation of prodrugs which can take advantage of plasma enzymes in vivo for regeneration of the parent molecule. A preferred prodrug in accordance with the invention is: where S-MP is 6-mercaptopurine.
US20100291158 Sustained release oral composition of an antipsychotic agent A sustained release oral composition of an antipsychotic agent comprising antipsychotic agent, λ-carrageenan and one or more pharmaceutically acceptable excipients; wherein the antipsychotic agent is 2-[2-(4-dibenzo{b,f}[1,4-thiazepin-11yl-1-piperazinyl)ethoxy ethanol] or its pharmaceutically acceptable salt.
WO2007025055A2 Benztropine compounds and uses thereof as dopamine uptake inhibitors Disclosed are benztropine analogs having the formula (I) in which Ar is a C6-C20 monocyclic aryl group or a C10-C20 bicyclic aryl group or a heteroaryl, heterocyclic, or arylheterocyclic group having 2 to 12 carbon atoms and one or more heteroatoms selected from the group consisting of N, O, S, P, and any combination thereof; m = 1 to 5; n = 1 to 3; and R1 to R4 are as described in the specification; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions and use thereof, e.g., in treating mental disorders.
EP0844875B1 Use of basic l-carnitine and acyl derivatives for lowering ceramide levels The therapeutic use of basic amino acids, acylated basic amino acids and their pharmacologically acceptable salts is disclosed for the preparation of a medicament for the prophylaxis of illnesses or the therapeutic treatment of cellular disorders accompanied by high levels of ceramide.
US20100280056 Identification of subjects likely to benefit from statin therapy Methods are provided herein to determine if a subject is a candidate for treatment with an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCR). The method includes determining the presence of at least one polymorphism in the HMGCR gene in a sample from a subject. The presence of at least one polymorphism indicates that the subject is a candidate for treatment with a statin, for example to decrease risk of or treat cancer, cardiovascular disease, diabetes, obesity, inflammatory disease, or auto-immune disease.
US20100183736 Rehydration beverage The present invention relates to a composition for the relief of hangover symptoms and methods of treating hangover symptoms.
CN1944452A 2-phenoxy chromone heteroside compounds and its preparing method and use The present invention relates to one kind of 2-phenoxy chromone glycoside compound and its preparation process and use. The compound is separated from alpine yarrow herb, and is named chemically as 6-demethoxy-4'-O-methyl capillarisin-7-O-beta-D-glucoside. Its structure has been determined through physical and chemical constant measurement and spectral data analysis, and initial activity screening test proves its antiviral, immune suppressing and blood fat reducing activity.
US20060058381 Pharmaceutical formulation comprising (r)-bicalitamide The present invention relates to a pharmaceutical formulation comprising the drug 4′-cyano-α′,α′,α′-trifluoro-3-(4-fluorophenylsulphonyl)-2-hydroxy-2-methylpropiono-m-toluidide in a solid dispersion with an enteric polymer having a pKa from 3 to 6, wherein >50% of the drug is provided in the form of the R-enantiomer. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of an enteric polymer having a pKa from 3 to 6 in solid dispersion with the drug, wherein >50% of the drug is provided in the form of the R-enantiomer, for increasing the bioavailability of the drug; for reducing inter-patient variability in plasma concentrations of the drug; for enhancing the storage stability of the drug; or for treating and/or reducing the risk of prostate cancer in a patient.
US20110046141 Use of pde5 inhibitors for treating circadian rhythm disorders A method of altering circadian rhythm in a mammal is provided. In certain embodiments, the method comprising: administering to the mammal a PDE5 inhibitor, e.g., sildenafil, vardenafil, tadalafil or zaprinast. The method may be employed to prevent a circadian rhythm disorders including, but not limited to transmeridian flight disorder (i.e., “jet-lag”), shiftwork-related disorder, seasonal affected disorder and insomnia by phase delay or phase advance.
US8821934 Pullulan-containing powder, process for producing the same and use thereof The object of the present invention is to overcome conventional demerits of pullulan powders prepared by conventional techniques, i.e., they could not be homogeneously mixed with non-reducing saccharides composed of glucose units when mixed together, and the resulting mixtures do not easily dissolve in water; and to provide a pullulan-containing powder with an improved rate of water dissolution, as well as to provide preparations and uses thereof. The present invention solves the above object by providing a pullulan-containing powder which uniformly comprises pullulan as a main ingredient and a non-reducing saccharide, and their process and uses; wherein the pullulan-containing powder is prepared by the steps of preparing a solution dissolving pullulan and a non-reducing saccharide homogeneously, pulverizing the solution, and collecting the resulting pullulan-containing powder. The powder has an improved rate of water dissolution, while retaining satisfactory resistance to humidity without fear of causing separation between the pullulan and the non-reducing saccharide.
US20060128624 Pharmacokinetic and pharmacodynamic modeling of erythropoietin administration The present invention relates to systems and methods for obtaining optimized EPO dosage regimens for a desired pharmacodynamic/pharmacokinetic response. The system includes choosing one or more EPO dosage regimens, then using a PK/PD model to determine the pharmacodynamic/pharmacokinetic profile of one or more EPO dosage regimens, and finally selecting one of the EPO dosage regimens for administration to achieve the desired pharmacodynamic/pharmacodynamic response based on the EPO profile.
CN101348569A Organotin coordination polymeric compound, preparation and use thereof The invention discloses an organotin coordination polymer which has a structural formula showed in a figure. The preparation method comprises the following steps of: in the inert atmosphere, adding 2- thiophene acetic acid, sodium ethoxide and tributyl tin chloride into a benzene solvent in standard Schlenk tube in order; stirring the mixed solution for 12 to 14 hours at a temperature of between 38 and 42 DEG C, and carrying out filtering after the mixed solution cools down; distilling the mixed solution to dryness the achromatic solution obtained from the filtering through a rotary evaporograph to obtain white powder; carrying out recrystallization through the mixture of an ethyl ether and a petroleum ether to obtain achromatic crystal which is just the organotin coordination polymer. The polymer can be used for preparing medicines curing gastric cancer, nasopharyngeal carcinoma, hepatic carcinoma or leukemia.
CA2593582A1 Bendamustine pharmaceutical compositions The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases. Preferred solvent used in a pre-lyophilized composition of bendamustine is tertiary-butyl alcohol .
US20080317729 Ammonium Salts and Ammonium Salt/Mineral Salt Clathrate Compounds for Use as Vehicle and Effective Form for Pharmaco-Medical Applications and for Use as Phase Transfer Agents for Chemical Applications This invention relates to ammonium salts and stable storable ammonium salts and ammonium salt/mineral salt clathrate compounds (inclusion compounds, clusters) having acid dibasic anionic acid residues such as bicarbonate, to methods for producing them and to pharmaco-medical and chemical synthetic applications for said compounds. According to the invention, compounds for pharmaco-medical and chemical synthetic applications are produced which comprise the ammonium salt and ammonium salt/mineral salt clathrate compounds (inclusion compounds, clusters) having acid dibasic anionic acid residues of general formula I with R1, R2, R3 and R4=alkyl and substituted alkyl straight-chain or branched, optionally having an alcohol, ether, silyether, ester, amino or amide function, H or aryl-alkyl, with aryl being an aromatic or heteroaromatic ring having optionally additional substituents, such as alkyl having 1 to 4 C atoms, OH, NR*2 with R*2=O, alkyl with alkyl of between 1 and 4 C atoms or H, COOH, COOR, CN, NO2 and the cationic positive N+ is optionally part of an active agent, Y is a dibasic acid residue of an organic dicarboxylic acid or CO3 −, corresponding to HY−=HCO3 −, and x=0.5 to 30 represents the number of the mineral salt molecules for clathrate compound formation or 0. In pharmaco-medical applications applies the generalizable effectiveness principle according to which to ammonium salt/mineral salt cluster is used as vehicle and active agent for novel forms of application of nitrogen-containing active agent bases. In chemistry, these agents are used in the synthesis of active agents and valuable products, e.g. of cyclic carbonates.
WO2013139209A1 Topiramate sustained-release pharmaceutical composition, method for preparing same, and use thereof A topiramate sustained-release pharmaceutical composition comprising no binders. The topiramate sustained-release pharmaceutical composition is a sustained-release pellet, comprising a blank pill core, a medicament layer, and a sustained-release coating layer.
EP1773308A1 Combination of bupropion and a second compound for affecting weight loss Disclosed are compositions for affecting weight loss comprising bupropion and a second compound, where the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions, antagonizes cannabinoid receptor activity, or is useful in the treatment of bipolar disorders.. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual with a combination of bupropion and a compound that enhances α-MSH activity, antagonizes cannabinoid receptor activity, or is useful in the treatment of bipolar disorders.
CN102670596A Application of amidine compound The invention discloses application of an amidine compound which is represented as formula I and is used for preparing nicotinamide phosphoribosyl transferase inhibitors. The invention also discloses application of a compound I which is used for preparing medicines preventing and/or curing cancer. The application discovers novel use of the compound I, and the compound can inhibit well the activity of nicotinamide phosphoribosyl transferase, can be used for preparing medicines which prevent and/or cure diseases by inhibiting the nicotinamide phosphoribosyl transferase and also can be used for preventing and curing diseases such as cancer.
CN103224532A Cr(III) compound, and preparation method and application thereof The invention provides a Cr(III) compound, and a preparation method and an application thereof. The preparation method of the compound comprises the steps of adding Cr(III)Cl3.6H2O and 4,4'-methylene-bis(3-hydroxyl-2-naphthoic acid) to a reactor; dissolving the above materials by an organic alcohol; adding zinc granules, dropping in ethanediamine under a reflux state; reacting for 20-60 min continuously;, wherein 0.73 g of 4,4'-methylene-bis(3-hydroxyl-2-naphthoic acid), 0.1-1 g of the zinc granules, 10-30 mL of the organic alcohol and 0.5-1 g of the ethanediamine are added in every 1 g of Cr(III)Cl3.6H2O; cooling a reaction solution; and filtering to obtain a target product. The compound has good water solubility and a controlled-release function, is beneficial to absorption and can be used for preparing weight-reducing medicines.
US20110257267 Reducing the Risk of Pathological Effects of Traumatic Brain Injury The present disclosure provides methods and compositions for reducing the risk of pathological effects of traumatic brain injury.
EP1173217B1 Enhanced delivery of nucleic acid-based drugs The invention provides methods and associated compositions for enhancing the intracellular delivery of a nucleic acid-based drug, such as an oligonucleotide or gene, by administering the nucleic acid-based drug in combination or sequentially with an enhancer. Preferred enhancers are caprylic acid, capric acid or their pharmaceutically acceptable salts. The preferred route of administration is oral.
US20110263588 Tricyclic compounds as glutamate receptor modulators The present invention relates to compounds that may be negative allosteric modulators of metabotropic receptors-subtype 5, and methods of making and using same.
WO2008080924A1 Use of 10-[(3r)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10h-phenothiazine for the preparation of a drug having a selective inhibition of muscarinic m1, m2 and m3 receptors The present invention relates to the use of 10-[(3R)-1- azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine as well as its pharmaceutically acceptable salts for the preparation of a drug having the particularity of treating or preventing urinary incontinence, by local and/or oral route.
US20120316152 Substituted isoquinolineand isoquinolinone derivatives A method for the treatment or prevention in a mammal of a disease associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase comprising administering to the mammal in need thereof at least one compound of the formula (I)
CN101732514A Medicament for treating rheumatism, rheumatoid arthritis, cervical osteoarthritis and lumbar osteoarthritis The invention discloses a medicament for treating rheumatism, rheumatoid arthritis, cervical osteoarthritis and lumbar osteoarthritis, which consists of the following components: (1) 12 to 21g of cooked tuber fleeceflower root, (2) 12 to 21g of twotooth achyranthes root, (3) 12 to 21g of obscured homalomena rhizome, (4) 12 to 21g of schizophragma root bark, (5) 32 to 56g of dried red date, (6) 160 to 280g of early brown sugar, and (7) 600 to 1,050 ml of white liquor. The medicament has the advantages of simple adopted components, readily available raw materials, greatly reduced cost, and is suitable for all the patients with the rheumatism, the rheumatoid arthritis, the cervical osteoarthritis and the lumbar osteoarthritis.
US20120178747 Compositions and methods for bone formation and remodeling The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm. Together with the observation that osteoblast cells produce autocrine canonical Wnt, Wnt7b, and that osteocytes produce paracrine Dkk1, we believe that the G171V mutation may cause an increase in Wnt activity in osteoblasts by reducing the number of targets for paracrine Dkk1 to antagonize without affecting the activity of autocrine Wnt.
US8173665 I-pheny 1-3,4-dihydropyrimidin-2(1H)-one derivatives and their use The invention relates to 4-cyanophenyl, 2-sulfanyl, 1-phenyl pyrimidine derivatives, processes for their preparation, and pharmaceutical compositions of the same. Compounds and compositions of the invention are useful in the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction, and heart failure development.
WO2012047287A2 Upregulation of opioid receptors for pain management Disclosed are methods for treating pain in a subject. The method includes upregulating expression of opioid receptors in the subject's dorsal root ganglion or trigeminal neurons. Also disclosed are methods of treating neuropathic and/or chronic pain in a subject. The method includes upregulating expression of μ-opioid or δ-opioid receptors in the subject's dorsal root ganglion or trigeminal neurons.
CN102178068A Application method of feed additive for lowering incidence rate of urinary calculi in sheep The invention provides an application method of a feed additive for lowering the incidence rate of urinary calculi in sheep. In the method, a hydrochlorothiazide tablet is taken as an additive and fed to the sheep based on addition amount of 3.0-6.0mg/kg per day, and a diuresis effect can be achieved within 10-30 days so that the incidence rate of the urinary calculi in the sheep is lowered to below 5%. By adopting the feed additive, the urine excretion amount of the sheep can be improved by over 35%. The selected hydrochlorothiazide tablet is a diuretic without toxic side effect; and the method for feeding the additive to the sheep is scientific and reasonable and easy for operation.
US20090317428 Immunogenic T-Helper Epitopes From Human Tumour Antigens and Immunotherapeutic Methods Using Said Epitopes The present invention relates to immunotherapeutic methods, and molecules and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer, in particular renal cancer. The present invention furthermore relates to tumour-associated T-helper cell peptide epitopes, alone or in combination with other tumour-associated peptides, that serve as active pharmaceutical ingredients of vaccine compositions which stimulate anti-tumour immune responses. In particular, the present invention relates to 338 novel peptide sequences derived from HLA class II molecules of human tumour cell lines which can be used in vaccine compositions for eliciting anti-tumour immune responses.
US20050053654 able to disintegrate in buccal cavity upon contact with saliva by formation of an easy-to-swallow suspension, in less than 60 seconds, containing fexofenadine or its salt and a binder, in the form of a coated granule, and excipients such as disintegrating agent, a soluble diluent, and a lubricant The present invention concerns orodispersible tablets, which are able to disintegrate in the buccal cavity upon contact with saliva by formation of an easy-to-swallow suspension, in less than 60 seconds, preferably in less than 40 seconds, containing fexofenadine in the form of coated granules, and a mixture of excipients comprising at least one disintegrating agent, a soluble diluent agent, a lubricant and optionally a swelling agent, a permeabilising agent, sweeteners, flavoring agents and colors; the process for obtaining such orodispersible tablets and the coated granules incorporated therein and the use of said orodispersible tablets in the treatment of seasonal allergic rhinitis.
EP2120974A1 Self-assembling amphiphilic polymers as antiviral agents There are provided amphiphilic biodegradable copolymers comprising a hydrophilic backbone with pendant aliphatic groups as the hydrophobic component. The polymers form nanoscale molecular aggregates in aqueous environments, which have hydrophobic interiors that are capable of solubilizing insoluble organic compounds and disrupting viral coat proteins. The polymers optionally feature reactive functional groups that provide attachment points for antibodies, ligands, and other targeting moieties which mediate adherence of the aggregate to a viral target.
US20080221021 Novel Corticotropin-Releasing Factor Receptor 1 (Crfr1) Agonist The present invention relates to a compound which is highly selective for CRFR1 without having any significant cross-reactivity for corticotropin-releasing-factor-receptor-2 (CRFR2) and/or corticotropin-releasing-factor-binding protein (CRFBP), said compound comprising or alternatively consisting of the amino acid sequence as depicted in SEQ ID No: 1. In another aspect, the present invention relates to a pharmaceutical and/or diagnostic composition comprising the novel CRFR1 agonist of the present invention. The present invention also provides a kit comprising the novel CRFR1 agonist of the present invention and optionally instructions to use. Furthermore, the present invention provides the use of the compound of the present invention for the preparation of a pharmaceutical composition for the treatment of depression and, additionally, the use of the compound of the present invention for the preparation of a diagnostic composition for the determination of pituitary corticotroph responsiveness and/or for differentiating pituitary and ectopic production of ACTH in patients with ACTH-dependent Cushing's syndrome.
WO2006014903A3 Compositions and methods of use for adam12 antagonists in treating disease Microarray analysis, confirmed by RT-PCT, demonstrated that lung squamous cell carcinoma, colon/colorectal cancer, and breast carcinoma mRNA hybridizes specifically and preferentially to ADAM12L. Microarray analysis also demonstrated that RNA from malignant bladder, pancreas, and stomach tissue hybridizes specifically to ADAM12. ADAM12L is a transmembrane protein overexpressed on the surface of cancer cells compared to normal tissues and thus provides a therapeutic target for treating cancer. Modulators of ADAM12, highly expressed in cancerous as compared to normal tissues, are provided for the diagnosis and treatment of proliferative disorders such as cancer and psoriasis. The invention further provides methods of treating cancer with therapeutic agents directed toward ADAM12.
WO2006113853A2 Topiramate compositions for treatment of headache A composition containing from about 10 to about 50 mg of topiramate in combination with one or more of parthenolide, magnesium and riboflavin is effective for treating headaches, and particularly migraine headaches, while reducing or eliminating the side effects experienced by users of prior higher dose topiramate compositions.
US20100255086 Method for oral mucosal absorption of acetyl salycylic acid A method for delivering acetyl salicylic acid to an individual via oral mucosal absorption by providing a melting capsule which includes a therapeutic amount of an acetyl salicylic acid; and administering the capsule sublingually in the patient such that the capsule melts at the individual's body temperature and delivers the acetyl salicylic acid directly into the bloodstream of the individual quickly and without complications; and a melting capsule comprised of a material that has the same melting point as the human body temperature and includes a therapeutic amount of an acetyl salicylic acid liquid or powder having a pH in the range of 2 to 7.
WO2006092573A1 Indazolylamino qionazoline derivatives as antitumor agents A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.
CN102836172A Powder combination containing glucose The invention relates to a powder combination containing glucose and a preparation method of the powder combination. Particularly, the powder combination contains glucose, halogeno salts of potassium, halogeno salts of sodium and the like. The powder combination achieves favorable pharmaceutical performance.
CN102988554A Foot therapy massage cream The invention relates to a foot therapy massage cream. The foot therapy massage cream comprises the following components in parts by weight: 14-16 parts of salicylic acid, 8-13 parts of safflower, 5-7 parts of amur corktree bark, 4-9 parts of dahurian angelica root, 7-10 parts of Mongolian snakegourd root, 6-14 parts of thinleaf milkwort root-bark, 9-18 parts of liquorice root and the balance of water. According to the foot therapy massage cream disclosed by the invention, medicines can infiltrate into foot skin very quickly, effectively stimulate various foot acupuncture points, promote blood circulation and reach the purpose of health care.
US20090324553 Chimeric Viral Envelopes The invention relates to chimeric polytropic viral envelope polypeptides and uses thereof, as well as to polynucleotides encoding said chimeric polypeptides and constructs comprising said polypeptides and/or polynucleotides. The invention also relates to chimeric retroviral envelope polypeptides, polynucleotides and vectors encoding said chimeric retroviral envelope polypeptides, virus particles and cells harbouring said chimeric envelope polypeptides. Said chimeric polypeptide comprise an envelope polypeptide, or fragment thereof, and a polypeptide sequence of a receptor binding region, ligand or polypeptide sequence of a ligand binding region, and optionally a linker sequence. The invention include methods of targeting receptors, methods of treatment and methods for delivery of agents using said chimeric retroviral envelope polypeptides. The invention is applicable for directed targeting and controlled fusion of virus particles with other cellular membranes.
US20120122806 Method of lowering glycemic index of foods A method of delaying digestion by an animal or a human of carbohydrates in food, comprising administering an effective amount of one or more flavonoids to the animal or human in conjunction with the food, wherein the flavonoids are selected from luteolin, apigenin, tricin and their pharmaceutically acceptable analogues and derivatives.
US20100189819 Neuro-degenerative inhibitor, neuro-endocrine modulator, and neuro-cerebral metabolism enhancer Neuro-metabolic and endocrine-function regulating/modulating compositions, are disclosed. The compositions of the present invention comprise Selegiline Hydrochloride, Procaine Hydrochloride, Vinpocetine, trimethylglycine, and an ingredient selected from a group consisting of N-nicotinoyl-gamma-aminobutyric acid (N-GABA), niacin, niacinamide, gamma-aminobutyric acid (GABA), and combinations thereof. Methods of using the compositions, compositions, and compositions of the present invention are also disclosed.
WO2014115488A1 Pharmaceutical composition for diseases caused by pathogenic microorganisms such as candida An object is to provide means for precisely treating vaginitis caused by intracellular parasite, protozoa, and/or fungus. A pharmaceutical composition for vaginitis, comprising a compound represented by the following general formula (1) as an active ingredient: (1) (In the formula, R represents a halogen atom or a hydrogen atom, and X represents a halogen atom.)
WO2006096802A1 Amorphous tegaserod maleate Provided are amorphous and purely amorphous tegaserod maleate and processes for the preparation thereof. Also provided are pharmaceutical compositions comprising amorphous or purely amorphous tegaserod maleate and methods for the treatment of irritable bowel syndrome using the same. (I)
US20080118441 Nutraceutical; omega fatty acids; mucilaginous fiber; no glutamine; gastroesophageal reflux disease, heartburn, acid indigestion, constipation, irritable bowel syndrome Gastrointestinal conditions, such as gastroesophageal reflux disease, heartburn, acid indigestion, constipation, irritable bowel syndrome, stomach and intestinal ulcers, gastrointestinal tract inflammation, thrush, diverticulitis, ulcerative colitis, Crohn's disease, diarrhea and cancers of the esophagus, pancreas, stomach, intestines and colon, may be treated or prevented by administration of compositions containing a therapeutically effective amount of a fatty acid and a therapeutically effective amount of mucilaginous fiber. Fatty acids suitable for use in the compositions include omega-3 fatty acids, omega-6 fatty acids and/or omega-9 fatty acids.
CN102516384A MLKL protein and application of MLKL protein as target point of cell necrosis inhibitor The invention discloses MLKL protein and an application of the MLKL protein as a target point of a cell necrosis inhibitor. The invention provides the protein represented by the following: (a) the protein comprises the amino acid sequence represented by the sequence 1; (b) the protein comprises the amino acid sequence represented by the sequence 13; (c) the protein is obtained through mutation of threonine on site 357 of the N terminal of the sequence 13 into alanine; (D) the protein is obtained through mutation of serine on the site 358 of the N terminal of the sequence 13 into alanine; (E) the protein comprises the amino acid sequence from the site 179 of the N terminal of the sequence 1 to the site 471 of the N terminal of the sequence 1. The protein is combined with RIP3 protein to provide an apoptosis effect, such that the protein can be used as the target point of anti-apoptosis drugs, and used for screening and developing the anti-apoptosis drugs. The invention further provides compounds for inhibitions of the nucleic acid expressed by the gene and the protein, wherein the compounds can be used as products for inhibitions of the apoptosis. The MLKL protein of the present invention provides important values for medical research and drug development.
EP1319009B1 Intermediates in cephalosporin production Cefuroxime in the form of a salt with n-butylamine; and its use for the production of cefuroxime axetil or for the production of the sodium salt of cefuroxime.
CN101967105A Beta-hydroxy protected didecyl quaternary ammonium salt with anticancer activity and preparation method thereof The invention relates to the synthesis of an emodin derivative with anticancer function, in particular to beta-hydroxy protected didecyl quaternary ammonium salt with anticancer activity and a preparation method thereof. The didecyl quaternary ammonium salt is methyl didecyl-[2-(4,5-dihydroxy-7-methoxy-9,10-anthraquinonyl)methyl] ammonium salt and is prepared from emodin serving as a raw materialthrough a series of synthetic reactions. In the invention, the emodin derivative has proliferation inhibiting functions with different degrees for five cancer cells such as liver cancer HepG2, gastric cancer BGC, neuroma SH-SY5Y, gastric cancer AGS and cervical cancer Hela and the normal human embryonic lung fibroblast HELF, and can be used for preparing medicaments for treating cancers.
CN103349697A Natural medicine extractive and preparation method and uses thereof The invention relates to a natural medicine extractive and a preparation method and purposes thereof. The natural medicine extractive is prepared from phellodendron amurense pericarpium citri reticulatae water decocted condensed extractives, phellodendron amurense ethyl acetate extractives and nobiletin according to the ratio of (2-8):(1-5):(5-7). The composition has a great curative effect on cancer chemotherapy related diarrhea, and meanwhile has a synergistic effect on cancer chemotherapy.
WO2011014475A3 Treating negative symptoms of schizophrenia associated with defective neuregulin 1 Use of a compound that is a serotonin transporter inhibitor, a selective norepinephrine reuptake inhibitor, or a 5-HT1A agonist for alleviating negative symptoms in a schizophrenia patient who carries a defective neuregulin 1 gene.
CN103417552A Veterinary aditoprim (ADP)-sulfamethoxazole (SMZ) compound injection and preparation method thereof The invention belongs to the technical field of preparation of veterinary drugs and particularly relates to a veterinary aditoprim (ADP)-sulfamethoxazole (SMZ) compound injection and a preparation method thereof. The injection comprises effective ingredients of ADP and SMZ of which the concentrations by weight/volume percent are respectively 2% and 10%. Propylene glycol serves as a cosolvent of which the concentration by weight/volume percent is 50% in the injection always; water for injection serves as a solvent; anhydrous sodium thiosulfate serves as an anti-oxidant of which the concentration by weight/volume percent is 0.15% always. ADP and SMZ are salified with an additive at first, then various auxiliary materials and the inject solvent are added, the mixture is continually stirred to be uniformly mixed and then subjected to rough filtration and fine filtration, after that, filling and sealing are performed quickly, sterilization under hot press is carried out for 20 min, and finally, leak detection, light inspection and the like are performed to obtain the veterinary ADP-SMZ compound injection. The injection has a simple preparation process, the quality meets the requirements specified in pharmacopeia, a long-acting slow release effect can be taken, and the injection is suitable for treating digestive and respiratory tract infection of livestock, caused by sensitive bacteria.
WO2009106850A1 Anti-oxidants for use for the treatment of damage to bodily tissue An orally-administrable medicament for the treatment of damage to body tissues, particularly surface tissues, and especially tissues of the eye such as the retina and the corneal endothelium, comprises an anti-oxidant reagent. The anti-oxidant reagent may comprise one or more anti-oxidant compounds and/or precursors convertible within the body to anti-oxidant compounds. Vitamins, such as vitamin A, C and/or E, are particularly suitable. Selenium and/or zinc compounds may also be present. Dosages are preferably significantly greater than an RDA of the anti-oxidant compound and close to the MDA. The medicament may be used to treat medical conditions or tissue damage resulting from surgical or medical treatment. In the latter case, it may be administered before, during and/or after the surgical or medical treatment. A corresponding topically-administrable medicament may also be applied.
WO2011086424A1 Pharmaceutical use of multicyclic compounds mixtures as concomitant anti-cancer, anti-inflammatory and anti-pain agents This invention refers to a pharmaceutical use of a mixture of multicyclic compounds, namely ingenol and lanosta-8,24-dien-3-ol compounds, as concomitant anti-cancer, anti-inflammatory and anti-pain agents.
CN102803225A Imidazole derivatives and their use as modulators of cyclin dependent kinases The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+-O- or CR3; Y is N, N+-O- or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
US8349848 Pyrrolo[3,2-D]pyrimidines that are selective antagonists of A2B adenosine receptors The present invention provides compounds of the following formula and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
WO2006134600A1 Compounds useful for treating bipolar disorders The invention relates to the use of valnoctamide (VCD) for the treatment of bipolar disorder and in particular for the treatment of the manic phase of the bipolar disorder.
CA2737025C Lipid based pharmaceutical preparations for oral and topical application; their compositions, methods, and uses thereof The present invention relates to the topical and oral delivery of a composition comprising one or more active agents for treating a disease or symptoms in a subject. In some embodiments, the present invention comprises a composition comprising at least one active compound, e.g., finasteride or minoxidil, and one or more lipids. In some embodiments, the present invention relates to composition and method of preparation for treating androgenic alopecia (AGA), prevention of hair loss and female hirsutism. In some embodiment, the present invention comprises finasteride and at least one lipid component for the treatment of benign prostatic hyperplasia. In some embodiment, the present invention comprises tacrolimus or amphotericin B and at least one lipid component for the treatment of skin or eye related diseases. The present invention provides a method of preparation of a composition comprising at least one active compound and at least one lipid and administering the composition to a subject by oral or topical delivery. In certain embodiments the subject is a mammal. In certain preferred embodiment, the subject is human.
EP2177525A1 Metal complex compound, cancer therapeutic composition comprising the metal complex compound as active ingredient, and intermediate for production of the metal complex compound A metal complex compound which exhibits a high degree of adsorption to bone or inhibition of cell growth, and is highly effective for therapy of a cancer metastasized to bone and therapy of the primary carcinoma thereof; a therapeutic agent composition for a cancer containing as an active ingredient the metal complex compound or a physiologically acceptable salt thereof; and an intermediate for the metal complex compound are provided. More concretely, a metal complex compound represented by the following General Formula (1): (wherein R1 independently represents C1-C10 alkyl which may be branched or have a substituent; or a C3-C30 cyclic group which may have a substituent; and X represents CHR2, an oxygen atom or NR5); a therapeutic agent composition for a cancer containing it as an active ingredient; and an intermediate for the metal complex compound are provided.
CN102961610A Topical paste patch The invention discloses a topical paste patch which is prepared from angelica root, tuckahoe, radix scutellariae, radix paeoniae rubra, astragalus, twotooth achyranthes root, rhizoma coptidis, eupolyphaga, rhizoma corydalis, radices sileris, scorpio, safflower, rhizoma ligustici wallichii, angelica dahurica, snakeskin, frankincense, myrrh, camphor, herba schizonepetae, dangshen, radix rehmanniae praeparata, periostracum cicada, dipsacus root, caulis spatholobi, peach kernel, acacia catechu, nux vomica, costus root, radix bupleuri, croton, radix paeoniae alba, momordica cochinchinensis, giant knotweed, gastrodia elata, alseodaphne hainanensis, honeysuckle, eucommia bark, spurge, lithargite, sesame oil in specific proportion by virtue of a conventional method. The topical paste patch provided by the invention is unique in formulation, is reasonable in compatibility of medicines, has the efficacies of dredging collaterals and activating blood, dispelling the wind and relieving swelling, drawing out toxicity and easing pain, restraining hyperplasia, activating blood and dissolving stasis, promoting granulation and relieving pain, bacteriostasis and anti-inflammation, moreover has rapid curative effect, short curative course, high treatment rate and convenience in application, has tiny skin irritation and wide application range, and can be used for achieving the total effective rate in treatment of 98%. The topical paste patch provided by the invention is suitable for hyperostosis, rheumatic arthritis, scapulohumeral periarthritis, lumbar disc herniation and the like.
WO2008051795A3 Preventing or reducing oxidative stress or oxidative cell injury by the administration of a water-insoluble cellulose derivative A water-insoluble cellulose derivative, such as ethyl cellulose is useful for preventing or reducing oxidative stress or oxidative cell injury in tissues of an animal and in particular for influencing the level Stearoyl-CoA Desaturase-1 (SCD1) gene expression or ATP synthase mitochondrial F1 complex assembly factor 1 (ATPAF1) gene expression in non-adipose tissues of the animal.
CN103340947A Natural medicine composition and preparation method as well as application thereof The invention relates to a natural medicine composition and a preparation method as well as an application thereof. The natural medicine composition is prepared from a concentrated extract of semen plantaginis and hawthorn which are decocted with water, as well as semen plantaginis polysaccharides and total flavonoids of the hawthorn according to the ratio of (4-8):(1-5):(5-7). The natural medicine composition has the excellent treatment effect on associated diarrhea caused by cancer chemotherapy and has the synergistic effect on the cancer chemotherapy at the same time.
EP2504339A1 Benzene-fused 6-membered oxygen-containing heterocyclic derivatives of bicyclic heteroaryls The invention relates to new derivatives of formula I, wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a proliferative disease.
CA2239053C Diphenyl pyridyl ethane derivatives as pde iv inhibitors The invention encompasses the novel compound of formula (I) useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of formula (I).
WO2014122474A1 Piperidin-1 -yl and azepin-1 -yl carboxylates as muscarinic m4 receptor agonists The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain.
CN102872032A Application of Gypensapogenin B in anti-hypoxia drugs The invention discloses an application of Gypensapogenin B in preparing anti-hypoxia drugs. The anti-hypoxia action of the Gypensapogenin B disclosed by the invention is observed through an integral and cellular level hypoxia model, and a result proves that the Gypensapogenin B can be used for remarkably increasing the survival rate and the survival time of asphyxiant hypoxia and acute decompression hypoxia mice and relieving myocardial damage of drug specificity hypoxia mice. The Gypensapogenin B is also remarkable in protective effect on hypoxia damage of myocardial cells and nerve cells of suckling mice cultured in vitro. The application of the Gypensapogenin B in preparing the anti-hypoxia drugs is provided.
US20120114737 Silicone acrylate hybrid composition and method of making same A silicone acrylate hybrid composition includes the reaction product of a silicon-containing pressure sensitive adhesive composition, an ethylenically unsaturated monomer, and an initiator. The silicon-containing pressure sensitive adhesive composition includes acrylate or methacrylate functionality. A method of making the hybrid composition includes polymerizing the ethylenically unsaturated monomer and the silicon-containing pressure sensitive adhesive composition in the presence of the initiator.
US20140087059 Pharmaceutical composition and process for montelukast tablets The manufacture of compositions containing montelukast and to stable tablet compositions resulting thereof are disclosed, which include a first compaction step of a dry blend including, montelukast or a pharmaceutically acceptable salt thereof, and microcrystalline cellulose, and a further compression step into tablets.
WO2007049137A3 Canola extracts containing high levels of sinapic acid Disclosed in certain embodiments is a canola extract comprising greater than 30% sinapic acid, pharmaceutical compositions thereof and methods thereof, wherein the canola extract is for use in treating cancer. Further disclosed are methods for extracting phenolic acids from canola meal.
CA2792601A1 Solid compositions of amorphous hcv inhibitors The present invention features solid compositions comprising amorphous Compound I. A solid dispersion of the present invention also contains a pharmaceutically acceptable hydrophilic polymer and a pharmaceutically acceptable surfactant. Compound I may be formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.
EP1124824B1 Chromenone and chromanone derivatives as integrin inhibitors The invention relates to compounds having formula (I), wherein R?1, R2, R3, R4, R5, R7, R8, R11¿, Z, m and n have the meaning cited in claim 1, and to the physiologically acceptable salts and solvates which can be used as integrin inhibitors, especially in the prophylaxis and treatment of circulatory diseases, in case of thrombosis, myocardial infarction, coronary heart diseases, arteriosclerosis, osteoporosis, pathologic processes caused or propagated by angiogenesis and in tumor therapy.
WO2006137433A1 Aqueous preparation having levocabastine solubilized therein A weakly acidic to almost neutral aqueous preparation containing levocabastine, a cyclodextrin and a water-soluble cellulose derivative. A conventional levocabastine suspension preparation needs to be fully shaken to give a homogenous solution before use. However, the inventive levocabastine preparation does not need such an effort since levocabastine is solubilized in the preparation. The levocabastine preparation can be applied to eyes in the form of an eye drop even when contact lens are worn, and therefore is easy to use for a user.
WO2007057687A1 Piperazine derivatives and their use in therapy Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors wherein R1 is a radical of formula -(Alk1)m-(NH)p-(Alk2)n-Q wherein m, n and p are independently 0 or 1, Alk1 and Alk2 are straight or branched chain divalent C1-C6 alkylene or C2-C6 alkenylene radicals, and Q is (i) hydrogen, except in the case where m, n and p are each 0, or (ii) an optionally substituted carbocyclic or heterocyclic group; R2 is hydrogen, C1-C3 alkyl, cyclopropyl, or -CF3; Ring A is a phenyl or 5- or 6-membered heteroaryl ring either of which is optionally substituted; Ar is a phenyl or 5- or 6-membered heteroaryl ring either of which is optionally substituted; L is -CH2-, -C(=O)-, -NH-, -O-, -S-, -SO-, -SO2-, -(CH2)2-, -CH=CH-, -OCH2-, -CH(CH3)-, or -NH-CH2-; s is 1 and W is an optionally substituted N-containing heterocyclic ring of 5 to 7 ring atoms; or s is O and W is an optionally substituted N-containing saturated heterocyclic ring of 5 to 7 ring atoms, or an N-containing heteroaryl ring of 5 or 6 ring atoms substituted by at least one substituent selected from amino, C1-C6 alkylamino or cyano; or a pharmaceutically acceptable salt, hydrate or solvate thereof.
CN101648926B Febuxostat crystal form and preparation method thereof The invention relates to a Febuxostat crystal form. The x-ray powder diffraction has characteristic peaks when a refraction angle 2 theta is at 6.80+/- 0.2 degree, 11.04+/- 0.2 degree, 13.56+/- 0.2 degree, 15.74+/-0.2 degree, 17.56+/-0.2 degree, 20.36+/-0.2 degree, 22.10+/-0.2 degree, 24.72+/- 0.2 degree, 25.38+/- 0.2 degree, 28.80+/-0.2 degree and 29.10 degrees+/- 0.2 degree. The invention also provides a preparation method of the Febuxostat crystal form. The crystal form has better stability and is suitable for technically applying preparations and being stored in a long period.
US20120045487 Multiphasic microfibers for spatially guided cell growth A multiphasic microfiber for a three-dimensional tissue scaffold and/or cellular support is provided in one aspect that includes at least one biocompatible material. The multiphasic microfiber optionally has a first phase and at least one distinct additional phase and is formed by electrohydrodynamic jetting. Further, such microfibers optionally have one or more biofunctional agents, which may be surface-bound moieties provided in spatial patterns. Multiphasic microfibers formed in accordance with the disclosure may form, in some cases, three-dimensional fiber scaffolds with precisely engineered, micrometer-scaled patterns for cellular contact guidance, which may thus support and/or promote cellular growth, proliferation, differentiation, repair, and/or regeneration for tissue and bioengineering applications.
WO2009130453A1 Inhibitors of plk Compounds of formula (I) are PLK inhibitors, useful for the treatment of cell proliferative diseases: wherein R1 is hydrogen, or an optionally substituted (C1-C6)aIkyl, (C2-C6)alkenyl, (C2- C6)alkynyl or (C3-C6)cycloalkyl group; R2 is hydrogen, or an optionally substituted (C1- C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R3 is hydrogen, -CN, hydroxyl, halogen, optionally substituted (C1C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl, -NR5R6 or C1-C4 alkoxy, wherein R5 and R6 are independently hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted mono- or bi-cyclic carbocyclic or heterocyclic ring or a ring system having up to 12 ring atoms; T is a radical of formula R-L1-Y1- wherein L1 and Y1 are as defined in the claims and R is an carbon-linked, alpha alpha disubstituted amino acid or amino acid ester residue.
CN101778619B Gel-like composition for external application comprising adenine compound Disclosed is a composition for external application, which can be applied on a part of the skin to more effectively elicit the useful activity of an adenine compound such as adenine, adenosine and a phosphate ester of adenosine, and which has an excellent long-acting property and an enhanced skin-moisturizing effect. A gel-like composition for external application which contains an adenine compound such as adenine, adenosine and a phosphate ester of adenosine is prepared by using agar as a gelling agent. The gel-like composition for external application is further prepared into the form of a sheet-like adhesive skin patch. The gel-like composition for external application, which is in the form of a sheet-like adhesive skin patch, is kept in the state immersed in an aqueous solution containing the adenine compound.
CN102665750A Nutritional composition beneficial to small intestine Studies were conducted on cytokine production in the small intestine and spleen and on damage to the small intestine of a group of ConA-induced hepatitis model mice that ingested a nutritional composition beneficial to the small intestine. As a result, in the group of mice that ingested the nutritional composition beneficial to the small intestine, inhibition of a rise in MCP-1 and IL-6 production in the small intestine and spleen was confirmed in addition to inhibition of a rise in liver and plasma cytokine production, and a reduction in small intestine tissue damage was displayed. The nutritional composition beneficial to the small intestine was evaluated by measuring the small intestine and large intestine weights of normal mice after two weeks of ingestion. As a result, there was an increase in the small intestine and large intestine weights, and the average length of the intestinal villi and thickness of the muscularis propria were significantly higher than in the control group.
WO2006052496A8 Compound useful for the treatment or prevention of cognitive disorders associated with diabetes and the use thereof Described is the efficient synthesis of an easy to manipulate and utilize, soluble tartrate salt of a potent, reversible butyrylcholinesterase inhibitor, (-)-(3aS)-3a-methyl -1,2,3,3a,8,8a-hexahydropyrrolo-[2,3-b]indol-5-yl N-4'-isopropylphenylcarbamate ('MHI tartrate'), for use in altering the enzymatic activity of butyrylcholinesterase and/or acetylcholinesterase in a subject exhibiting or predicted to exhibit cognitive disorders associated with diabetes. Subjects may be suffering from or predicted to suffer from abnormal acetylcholinesterase and/or butyrylcholinesterase activity levels or from an inability to metabolize or catabolize blood sugar normally. The method comprises administering to the subject an effective amount of MHI tartrate dispensable in discrete pharmaceutically useful dosages. MHI tartrate effectively inhibits both acetylcholinesterase and butyrylcholinesterases and additionally is highly selective for butyrylcholinesterase over acetylcholinesterase.
US20090263443 Methods for treating post-operative effects such as spasticity and shivering with clondine Effective treatments of spasticity and shivering that accompanies surgeries are provided. Through the administration of an effective amount of clonidine at or near a target site, one can relax muscle fibers. This administration of clonidine or a pharmaceutically acceptable salt thereof is particularly useful following the surgery.
CN103070867A Metformin-nicotinic acid combined drug for treating non-alcoholic fatty liver disease The invention relates to a pharmaceutical composition and especially relates to a metformin-nicotinic acid combined drug for treating the non-alcoholic fatty liver disease. The metformin-nicotinic acid combined drug comprises biguanide hypoglycemic drugs or their pharmaceutically acceptable salts, wherein the biguanide hypoglycemic drugs comprise metformin, phenformin and buformin. The metformin-nicotinic acid combined drug also comprises a nicotinic acid fat-reduction drug and medicinal carriers. The metformin-nicotinic acid combined drug is used for treating the non-alcoholic fatty liver disease.
WO2013124381A1 Peltatin for use in the treatment of metabolic disorders The present invention relates to the field of metabolic disorders and aims to identify natural compounds that can be used effectively in this field. In particular, the present invention provides a composition comprising at least one peltatinfor use in the treatment or prevention of metabolic disorders or risk factors thereof.
US20110152746 Methods for generating new hair follicles, treating baldness, and hair removal The present invention provides methods of treating baldness in a subject and generating new hair follicles, comprising epidermal disruption and administration of a compound that promotes a differentiation of an uncommitted epidermal cell into a hair follicle cell. The present invention also provides methods for hair removal and inducing hair pigmentation.
CN103405466A Compound synergistic tylosin tartrate The invention relates to a compound synergistic tylosin tartrate. The invention aims to provide an compound synergistic tylosin tartrate for injection for livestock, which has quick and definite curative effect on livestock and fowl respiratory system infections and complications. The medicine is composed of the following components in parts by weight: 1 part of tylosin tartrate, 1 part of kanamycin sulfate, 0.2 part of trimethoprim, 0.2 part of cosolvent and 0.05-0.1 part of pain relieving agent. The cosolvent is citric acid or succinic acid or compound of both, and the pain relieving agent is procaine hydrochloride or lidocaine hydrochloride or compound of both. The compound synergistic tylosin tartrate for injection for livestock contains the three pharmaceutical components, including tylosin tartrate, kanamycin sulfate and trimethoprim. The invention solves the problem of incapability of well controlling the secondary infection due to the narrow antimicrobial spectrum of the tylosin tartrate in treating mycoplasma infection, solves the problem of insolubility of trimethoprim in water, has a synergistic effect on tylosin tartrate and kanamycin sulfate, and is accurate in dosage and convenient to use.
US20080234271 Arylphenylamino- and Arylphenylether-Sulfide Derivatives, Useful For the Treatment of Inflammatory and Immune Diseases, and Pharmaceutical Compositions Containing Them The present invention relates in part to compounds of formulas (I) and (III): and pharmaceutically-acceptable salts and prodrugs thereof. These compounds can be useful for treating diseases such as inflammatory and immune diseases. The present invention also relates to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a subject.
WO2005032514A1 Transdermal pharmaceutical composition The invention relates to a liquid crystal gel containing polyoxyethylene-glyceryl-trioleate, propylene-glycol, isopropyl myristate and a hyaluronic acid salt or complex for use in the manufacture of transdermal pharmaceutical compositions and healing cosmetics. The invention also relates to transdermal pharmaceutical composition consists of an estrogen and a progestin component as well as a liquid crystal gel containing polyoxyethylene-glyceryl-trioleate, propylene-glycol, isopropyl myristate and a hyaluronic acid salt or complex. The invention can be applied for transdermal hormone replacement therapy and for other transdermal depending on the active principles included.
CN102895247A Application of Houttuynoid B to medicament for treating oophoroma The invention discloses an application of Houttuynoid B to preparation of a medicament for treating human oophoroma, belonging to the technical field of novel medicament applications. As proved by in-vitro MTT (Methyl Thiazolyl Tetrazolium) antitumor activity evaluation, the Houttuynoid B has remarkable inhibiting effects on the growth of human oophoroma cell strains HO-8910, HOC1 (Hepatic Oval Cell 1) and OVAC. Therefore, the Houttuynoid B can be used for preparing a medicament for resisting oophoroma, and has good development and application prospects. The application of the Houttuynoid B to preparation of a medicament for treating human oophoroma related to the invention is disclosed for the first time. A framework type belongs to a brand new framework type, and the inhibiting activity of the Houttuynoid B on human oophoroma cells is unpredictably high.
EP1938799A1 Methods and compositions for treating and preventing posterior segment ophthalmic disorders Methods and compositions for the prophylactic and therapeutic treatment of ophthalmic disorders associated with the posterior segment of the eye using topical ophthalmic compositions comprising therapeutic agents. The invention specifically provides for methods and compositions for the prophylactic and therapeutic treatment of retinal disorders associated with neovascularization using topical ophthalmic compositions comprising hydroxamic acid matrix metalloproteinase inhibitors such as batimastat.
US7045649 compounds are suitable, for example, for use as anorectics Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of embodiments of the invention may include compounds of formula I in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for use as anorectics.
CN103446143A Application of Lycojaponicumin C in gastric cancer treatment drug The invention discloses application of Lycojaponicumin C in preparation of a gastric cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Lycojaponicumin C also has remarkable inhabiting effect on growth of human gastric cancer cell strains HGC-27, MGC-803, BGC-823 and SGC-7901. Therefore, the Lycojaponicumin C can be used for preparation of an anti-gastric cancer drug and has good development and application prospect. The application of the Lycojaponicumin C in the preparation of the gastric cancer treatment drug is disclosed for the first time. Due to the fact that the fact that the skeleton type is a novel skeleton type, and the high gastric cancer cell inhibiting activity of the Lycojaponicumin C is previously unimagined.
US20100310487 Active ingredient combination and use thereof An active ingredient combination which comprises a) glycerol monoalkyl ether, b) bispyridinium alkane, c) polyol and d) antioxidant. The combination is advantageously used for producing a preparation for the treatment of undesired body odour, for example for producing a cosmetic deodorant preparation, an antidandruff hair cleansing composition, a preparation for the treatment of blemished skin and acne or a preparation for the treatment of foot and/or skin fungus.
EP1539208A2 Compositions and methods for modulating physiology of epithelial junctional adhesion molecules for enhanced mucosal delivery of therapeutic compounds Compositions and methods are provided that include a biologically active agent and a permeabilizing agent effective to enhance mucosal delivery of the biologically active agent in a mammalian subject. The permeabilizing agent reversibly enhances mucosal epithelial paracellular transport, typically by modulating epithelial junctional structure and/or physiology at a mucosal epithelial surface in the subject. This effect typically involves inhibition by the permeabilizing agent of homotypic or heterotypic binding between epithelial membrane adhesive proteins of neighboring epithelial cells. Target proteins for this blockade of homotypic or heterotypic binding can be selected from various related junctional adhesion molecules (JAMs), occludins, or claudins. The permeabilizing agent is typically a peptide or peptide analog or mimetic, often selected or derived from an extracellular domain of a mammalian JAM, occludin or claudin protein.
CN101890003A Method for preparing novel chlorhexidine acetate cream The invention provides a method for preparing chlorhexidine acetate cream. The novel chlorhexidine acetate cream is prepared by adopting the micronization treatment technique, the content uniformity and the limit of impurities are better controlled, and the chlorhexidine acetate preparation having the advantages of high efficiency, quick effect and high stability and safety is provided by the method of the invention.
US20090099238 Use of a ppar-alpha agonist to treat patients suffering from weight gain associated with a ppar-gamma agonist treatment The present invention relates to the use of a pparα agonist to treat patients suffering from weight gain associated with a pparγ agonist treatment.
CN101856396B Dispersible tablet for treating hepatitis B and preparation method thereof The invention discloses a dispersible tablet for treating hepatitis B and a preparation method thereof. The dispersible tablet consists of silymarin, total saponin of cimicifuga dahurica, a diluent, a disintegrating agent, a lubricating agent, a flavoring agent, and a compatibilizer. The dispersible tablet has the advantages of good dispersed state, rapid medicament dissolution, high bioavailability, convenient administration, simple preparation technology, and no need of special equipment, and is suitable for mass production.
WO2013128029A1 Pharmaceutically active pyrazolo-triazine derivatives The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
CA2570047C 4-cycloalkoxy benzonitriles as androgen modulators The present invention is directed to a new class of 4-cycloalkoxy benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.
US8513188 Formulations comprising cyclic compounds This invention relates to the use of a cyclic compound of formula (I) wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (i) may comprise one or more double bonds; (ii) is optionally substituted; and/or (iii) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p·(n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulphur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p·(n+m) is selected from 3 to 30; wherein said compound is capable of forming a complex with a protonated primary and/or protonated secondary amino group and/or a protonated guanidinium group for the manufacture of a pharmaceutical or diagnostic composition.
WO2014023682A1 Multicomponent crystalline system comprising deferasirox and isonicotinamide and a process for the preparation thereof The present invention refers to a multicomponent crystalline system (co-crystal) comprising a compound of formula (1) (4-[3,5-Bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]benzoic acid; INN:Deferasirox) formula (1) and a compound of formula (2) (Isonicotinamide; pyridine-4-carboxamide) formula (2), as well as to a process for obtaining the same.
EP1861407A1 Thienopyridinone derivatives as macrophage migration inhibitory factor inhibitors Inhibitors of macrophage migration inhibitory factor having a thienopyridinone backbone are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with macrophage migration inhibitory factor activity. The inhibitors of macrophage migration inhibitory factor have the following structures formula (I), (II), (III) including forms such as stereoisomers, free forms, pharmaceutically acceptable salts or esters thereof, solvates, or combinations of such forms, wherein n, R1, R2, R3, X, and Y are as defined herein. Compositions comprising an inhibitor of macrophage migration inhibitory factor in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.
US20090258826 Pituitary adenylate cyclase activating peptide (PACAP) receptor (VPAC2) agonists and their pharmacological methods of use This invention provides novel peptides that function in vivo as agonists of the VPAC2 receptor. These insulin secretagogue polypeptides are shown to lower blood glucose in vivo more than controls upon glucose challenge. The polypeptides of this invention are also stable in formulation and have long half-lives. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, in particular type 2 diabetics. In particular, the invention is a polypeptide selected from a specific group of VPAC2-related polypeptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the insulin secretagogue peptides to said mammal. Also disclosed are methods of making the peptides, both recombinant and synthetic.
CN101869550A Oral sustained-release dry suspension taking clarithromycin as main ingredient The invention relates to oral sustained-release dry suspension taking clarithromycin as a main ingredient. The oral sustained-release dry suspension is prepared from the clarithromycin serving as the main active ingredient and pharmaceutically acceptable supplementary materials by pharmaceutical technology. The oral sustained-release dry suspension of the invention has the advantages of greatly increasing the patient compliance, reducing the number of missing taking medicine, along with stable and controllable quality, safety and effectiveness.
US7595403 Such as 3-Oxo-3H-benzo[d]isothiazole-2-carboxylic acid allylamide for treating hypercholesterolemia, hyperlipidemia, or atherosclerosis A novel class of benzisothiazole-3(2H)-one compounds is disclosed together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase mediated diseases. (I)
CN102846717A Disposable hand disinfection wet wipe A disposable hand disinfection wet wipe relates to the fields of daily living goods and medical care goods, and can solve problems comprising single sterilization principle and use inconvenience of present antiseptics and methods used for hand disinfection. The wet wipe comprises a wet wipe solution and a wet wipe solution carrier, wherein the wet wipe solution is prepared from 10-15wt% of isopropanol, 0.4-0.6wt% of didecyl dimethyl ammonium chloride, 0.5-1wt% of tea tree oil, 0.05-0.1wt% of disodium cocoamphodiacetate, 0.5-1wt% of glycerin, 0.1-0.5wt% of EDTA-2Na, 0.05-0.1wt% of jojoba oil, 0.5-1wt% of hydrogenated castor oil, and the balance water A disinfectant used in the invention is a compound of a double-chain quaternary ammonium salt, isopropanol and the tea tree oil, so a synergistic sterilization effect can be reached; and the use method of the wet wipe is simple, and used PET glue points can increase the surface friction coefficient, so the disinfecting sterilization purpose can be reached only through slight wiping, and the cleaning is thorough.
CN102846661A Compound nano-silver emulsifiable paste and preparation method thereof The invention discloses compound nano-silver emulsifiable paste and a preparation method thereof. The compound nano-silver emulsifiable paste is O/W or W/O type emulsifiable paste prepared from nano-silver and zinc oxide as main drugs by certain processes. Nano-silver has strong antibacterial effects and a wide antimicrobial spectrum and causes drug resistance of bacteria difficultly. Zinc oxide has convergence and wound heal promotion effects. The compound nano-silver emulsifiable paste prepared from nano-silver and zinc oxide has anti-infection and wound heal promotion effects. The compound nano-silver emulsifiable paste has treatment advantages of moisture exposed burn ointment and sulfadiazine silver cream and avoids treatment defects and adverse reactions of moisture exposed burn ointment and sulfadiazine silver cream. The compound nano-silver emulsifiable paste can be used for anti-infection treatment on burns and scalds, infected wounds caused by physical mechanical damages, and chronic surface ulcers, and promotion of wound heal. The compound nano-silver emulsifiable paste can also be used for treatment on skin diseases such as sores, carbuncles, furuncles, erysipelas and tinea caused by bacteria, fungi and viruses.
CN103570704A Quinazoline derivative with oxazolidinone ring side chain as well as preparation and application The invention discloses a quinazoline derivative which contains an oxazolidinone ring side chain and is as shown in formula I in the specification, or an enantiomer of the derivative. A target compound is prepared mainly by carrying out one-step condensing on 4-arylamine quinazoline as a nuclear parent and oxazolidinone formic acid. Tests show that the quinazoline derivative has a remarkable anti-proliferative effect on tumor cells associated with EGFR (Epidermal Growth Factor Receptor) tyrosine kinase activity in cellular level, such as human epidermoid carcinoma cell strain A431 over-expressing EGFR and Gefitinib-resistant human lung adenocarcinoma cell strain H1975, and particularly has a good inhibition effect on the drug-resistant cell strain H1975, so that the quinazoline derivative can be prepared into corresponding anti-tumor cell medicaments.
US20110190271 2,4-Pyrimidinediamine Compounds and Uses as Anti-Proliferative Agents The present invention provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferative diseases such as tumorigenic cancers.
WO2013036867A3 Compositions and methods for cancer and cancer stem cell detection and elimination In alternative embodiments, the invention provides compositions and methods for inhibiting or ablating cancer stem cells. In alternative embodiments, the invention provides compositions and methods for inhibiting the action of double-stranded RNA-specific adenosine deaminases, or ADAR, enzymes. In alternative embodiments, the invention provides compositions and methods for treating, ameliorating or preventing diseases and conditions responsive to the inhibition of cell differentiation and/or self-renewal of dysfunctional cells, cancer cells, leukemia cells, hematopoietic stem cells or cancer stem cells, e.g., leukemia or Chronic Myeloid Leukemia (CML). In alternative embodiments, the invention provides compositions and methods for inhibiting a Sonic Hedgehog (Shh) pathway, e.g., by using a Smoothened (SMO) protein inhibitor. In alternative embodiments, the invention provides compositions and methods for measuring or determining, or predicting, chronic myelogenous leukemia (CML) progression, Leukemic Stem Cell (LSC) generation and/or tyrosine kinase inhibitor resistance. In alternative embodiments, the invention provides compositions and methods for determining or measuring the effectiveness of a treatment, a drug, a therapy or a diet for eliminating, killing or reducing the amounts of a leukemic stem cell (LSC) or cells.
CN101579348A Application of 3,6'-disinapoyl sucrose (DISS) in preparing product for treating tristimania The invention discloses new medicinal application of 3,6'-disinapoyl sucrose (DISS), in particular the application of the 3,6'-disinapoyl sucrose (DISS) in preparing a product for treating tristimania. The 3,6'-disinapoyl sucrose (DISS) has better therapeutic effect on treating the tristimania caused by various reasons and obvious anti-depression activity to a pharmacological depression model, and the anti-depression activity of the 3,6'-disinapoyl sucrose is relative to the enhancement of the functions of 5-hydroxytryptamine (5-HT) and noradrenergic (NE) nerves. The DISS has no central excitation or inhibitive action within the range of an effective dosage of anti-depression.
CA2606945A1 An impurity of anastrozole intermediate, and uses thereof Reference markers and reference standards for the determination of impurities in Anastrozole are provided.
US20120046342 Oligonucleotide comprising an inosine for treating dmd The invention provides an oligonucleotide comprising an inosine, and/or a nucleotide containing a base able to form a wobble base pair or a functional equivalent thereof, wherein the oligonucleotide, or a functional equivalent thereof, comprises a sequence which is complementary to at least part of a dystrophin pre-m RNA exon or at least part of a non-exon region of a dystrophin pre-m RNA said part being a contiguous stretch comprising at least 8 nucleotides. The invention further provides the use of said oligonucleotide for preventing or treating DMD or BMD.
WO2006094209A3 N-benzimidazolylalkyl-substituted amide sirtuin modulators Provided herein are novel sirtuin-modulating compounds of formula ( Ia ) and methods of use thereof . The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
WO2009087667A3 Crystalline polymorphic forms of zopiclone, processes for their preparation and their pharmaceutical compositions Disclosed are processes for the preparation of crystalline polymorphic forms of zopiclone and their pharmaceutical compositions for use as a sedative.
CN103446149A Application of Lycojaponicumin C in small intestine peristalsis promoting drug The invention relates to application of Lycojaponicumin C in preparation of a small intestinal peristalsis promoting drug. A pharmacological experiment shows that the Lycojaponicumin C has good promoting effect on small intestinal peristalsis. The application of the Lycojaponicumin C in the preparation of the small intestinal peristalsis promoting drug is disclosed for the first time. Due to the fact that the skeleton type is a novel skeleton type and the high small intestinal peristalsis promoting activity of the Lycojaponicumin C is previously unimagined, the possibility that other compounds give any revelation does not exist, and the Lycojaponicumin C has outstanding substantive characteristics and meanwhile has a remarkable improvement in the preparation of the small intestinal peristalsis promoting drug obviously.
CN101810715A New application of fructus evodiae and extracts and compounds thereof The invention provides a new application of fructus evodiae and extracts and compounds thereof to prepare a medicament for treating hyperuricemia or/and gout. The invention also provides a medicinal composition prepared from effective dose of the fructus evodiae or extracts thereof as active components. The medicament comprises a fructus evodiae raw medicinal material, a solvent extract, total alkaloids of the fructus evodiae, single alkaloid of the fructus evodiae or a compound preparation containing the components, has the functions of blood uric acid reduction, anti-inflammation and analgesic activity, can be used for treating hyperuricemia and/or gout, has definite medicinal effect and high safety and provides a new medicine application selection for the clinics.
CN1771953A Medicine containing cepharanthine The present invention relates to five kinds of improved cepharanthine medicine preparation, including soft cepharanthine capsule, hard cepharanthine capsule, dispersed cepharanthine tablet, cepharanthine for injection and cepharanthine liquid for injection. These cepharanthine medicine preparations have the features of extracorporeal disintegration, complete absorption, high bioavailability and high clinical treating effect.
EP1697354A1 Isothiazole dioxides as cxc- and cc- chemokine receptor ligands Disclosed are novel compounds of the formula (IA): and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
US6891063 Salts with pharmaceutically acceptable organic bases, selected from ethylenediamine, ethanolamine, diethanolamine, lysine, benzyltrimethylammonium hydroxide and tetramethylammonium hydroxide; antiinflammatory agents, wound healing agents Salts of asiatic and madecassic acid with pharmaceutically acceptable organic bases, suitable for the preparation of pharmaceutical and cosmetic compositions for the topical and systemic treatment of erithema, varicose ulcers, venous insufficiency, bedsores, delayed cicatrization, ambustions, traumatic and surgery wounds, alloeosises of the cutaneous trophism, ophthalmic alloeosises and inflammatory processes.
US7901709 Active agent, a gel-phase lipid bilayer membrane of a phospholipid and a surface active agent contained in the bilayer membrane; increasing the percentage of active agent released at the phase transition temperature of the lipid bilayer A liposome contains an active agent and has a gel-phase lipid bilayer membrane comprising phospholipid and a surface active agent. The phospholipids are the primary lipid source for the lipid bilayer membrane and the surface active agent is contained in the bilayer membrane in an amount sufficient to increase the percentage of active agent released at the phase transition temperature of the lipid bilayer, compared to that which would occur in the absence of the surface active agent. The surface active agent is present in the lipid bilayer membrane so as to not destabilize the membrane in the gel phase.
US20100120868 Process For Preparing Solid Dosage Forms of Rosiglitazone Maleate The invention relates to a process for preparing a solid pharmaceutical composition rosiglitazone maleate, comprising the step of adsorption of rosiglitazone maleate onto carrier particles (C) during a dry mixing process.
CN102949724A Inhalation medicine composition containing glucocorticoid and NOS (nitric oxide synthase) inhibitor The invention discloses an inhalation medicine composition containing glucocorticoid and NOS (nitric oxide synthase) inhibitor, containing glucocorticoid which is used as an active ingredient, amino acid derivatives which are used as the NOS inhibitor, and one or more pharmaceutical excipients suitable for inhalation.
CN101978946A Application of new sodium houttuyfonate injection in treating milk cow mastitis The invention discloses a new sodium houttuyfonate injection and a preparation method thereof, which are used for treating milk cow mastitis and belong to the technical field of animal remedies. The sodium houttuyfonate injection comprises the following components in percentage by weight: 0.01 to 10 percent of new sodium houttuyfonate, 0.1 to 50 percent of solubilizing agent, 0.1 to 50 percent of pH modifying agent, and 0.01 to 0.5 percent of antioxidant. The preparation method comprises the following steps of: fully mixing the new sodium houttuyfonate with the solubilizing agent, and then uniformly grinding the mixture; adding aqueous solution of the antioxidant to adjust the pH to be 4.5 to 6.5; adding activated carbon to remove pyrogen; decarburizing and filtering the mixture; filtering the mixture for degermation by using 0.22 mum microporous filter membrane terminal; and performing nitrogen-filling and sub-package, capping sealing, and sterilized packaging to obtain the injection. The new sodium houttuyfonate injection has a simple formula, safe quality and high stability; and the preparation process is simple and feasible, is convenient to operate, is low in cost, is suitable for industrial production, and has an extensive prospect.
CN102198094A Artificial tear containing polyacrylic acid and sodium hyaluronate and preparation method thereof The invention discloses an artificial tear containing polyacrylic acid and sodium hyaluronate and a preparation method thereof. The artificial tear disclosed by the invention comprises polyacrylic acid, sodium hyaluronate, thickener, stabilizer, antioxidant, pH regulator, osmoregulator and de-ionized water. Based on the viscous synergetic effect generated by the combination of the polyacrylic acid and the sodium hyaluronate, the invention improves the bioavailability of the medicament and simultaneously reduces the total amount of polymers in the formula, thereby lowering the material cost, effectively reducing the in vivo retention volume of the polymers and enhancing the safety of the product. The artificial tear is prepared by a sterile operation process, thereby ensuring the sterile performance of the product, and enabling the product to be safer, more reliable, more convenient and more sanitary.
CA2387719C Azaindolizinone derivatives and cognitive enhancers comprising the same as effective components Azaindolizinon derivatives or pharmaceutically acceptable salts thereof represented by the formula I: (see formula I) wherein R1 represents hydrogen atom, halogen atom or C1-C6 alkyl, R2 represents hydrogen atom, C1-C6 alkyl, C1-C6alkoxy, hydroxy, halogen atom, amino, acetylamino, benzylamino, trifluoromethyl or -O- (CH2)n-R5 (R5 represents vinyl, C3--C8 cycloalkyl or phenyl, n being 0 or 1), R3 and R4 respectively represent C1-C6 alkyl or -CH(R7)-R6 (wherein R6 represents vinyl, ethynyl, phenyl (which may be substituted with C1-C6 alkyl, C1-C6 alkoxy, hydroxy, one or two halogen atoms, di C1-C6 alkylamino, cyano, nitro, carboxy or phenyl), phenethyl, pyridyl, thienyl or furyl and R7 represents hydrogen atom or C1-C6 alkyl) or R3 is coupled with R4 to form indan or dihydrophenalene.
EP1771180B1 Composition in the form of a spray comprising a combination of clobetasol propionate and calcitriol, an alcohol phase and an oily phase The invention relates to an anhydrous composition in the form of a spray comprising a combination of clobetasol propionate and calcitriol as pharmaceutical active ingredient, an alcohol phase and an oily phase in a physiologically acceptable medium, to the process for its preparation and to its use in cosmetics and dermatology.
CN103260627A Defibrotide for use in prophylaxis and/or treatment of graft versus host disease (gvhd). Defibrotide for use in prophylaxis and/or treatment of Graft versus Host Disease (GVHD) in humans is disclosed, preferably in hematopoietic stem cell transplantation (HSCT), more preferably allogeneic hematopoietic stem cell transplantation. Graft versus Host Disease of the invention (GVHD) can be acute aGVHD and/or chronic cGVHD, preferably acute.
CA2504755C Carbohydrate-based synthetic vaccines for hiv The present invention relates to a constructed oligosaccharide cluster, optionally bonded to an immunogenic protein, that can be administered to a subject to induce an immune response for increasing production of 2G12 and/or used in assays as reactive sites for determining compounds that inactivate and/or bind the high-mannose oligosaccharide cluster. Compositions comprising these clusters, methods of using these clusters and compositions are disclosed.
EP1043998B1 USE OF PYRAZOLO [3,4-b] PYRIDINE AS CYCLIN DEPENDANT KINASE INHIBITORS Compounds of formula (I) and pharmaceutically acceptable salts thereof for use as inhibitors of cyclin dependent kinases, wherein: X is O, S(O)m; Y is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl; R1 is hydrogen or lower alkyl; R2 is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocloalkylalkyl, -O-alkyl, -O-aryl, -NR4R5; R3 is hydrogen or lower alkyl; R4 is hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -O-alkyl, -O-aryl; R5 is hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, cycloalkyl, alkylcycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, -O-alkyl, -O-aryl; and m is 0, 1 or 2. The compounds of formula (I) are proteinkinase inhibitors and are useful in the treatment and prevention of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases.
CA2338206C High affinity ligands for nociceptin receptor orl-1 Compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is -CHO, -CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group; R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R2 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or-CO2(alkyl or substituted amino) or CN; Z2 is H or Z1; Z3 is H or alkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.
US7829595 A mixture of compound, e.g., cinacalcet hydrochloride and excipient in dosage form having a controlled dissolution profile , which comprises 50-125% of a target amount of theactive compound is released in 0.05 hydrochloric acid in 30 minutes; calcimimetics and calcilytics; hyperparathyroidism The present invention relates to a pharmaceutical composition comprising a therapeutically effective amount of a calcium receptor-active compound and at least one pharmaceutically acceptable excipient, wherein the composition has a controlled dissolution profile. The present invention further relates to a method of manufacturing the pharmaceutical composition, as well as a method of treating a disease using the pharmaceutical composition.
US7943184 Process for preparing an extract from ivy leaves The present invention relates to a process for preparing an extract from ivy leaves which includes the active ingredient hederacoside C and α-hederin, and to extracts prepared by this process. According to this there is initially provision of a first, α-hederin-rich extract and subsequently provision of a second, hederacoside C-rich extract. In a last step, the two extracts are blended to give an extract which has an adjusted hederacoside C content and an adjusted α-hederin content.
EP1509509A1 Glucagon antagonists/inverse agonists A novel class of compounds of the general formula (I), which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity. (I) wherein R2 is hydrogen or C1-6-alkyl, B is (II) Z is arylene or a divalent radical derived from a 5 or 6 membered heteroaromatic ring containing 1 or 2 heteroatoms selected from nitrogen, oxygen and sulfur.
WO2013120771A1 Imidazolylketone derivatives asd aldosterone synthase inhibitors The invention provides novel compounds having the general formula (I), wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds as inhibitors of aldosterone synthase.
WO2009020234A3 Pyrrolidin-2 -one derivatives as androgen receptor modulator A compound represented by the formula (I) according to claim 1 or a salt thereof has a superior androgen receptor modulating action.
CN102151265A Lansoprazole composition for injection The invention provides a lansoprazole composition for injection, containing lansoprazole and disodium ethylenediaminetetraacetate, wherein the weight ratio of the lansoprazole to the disodium ethylenediaminetetraacetate is 1:(0.02-0.1). The composition is prepared by the following steps: (1) medical liquid preparation: putting the lansoprazole and the disodium ethylenediaminetetraacetate into a preparation tank, adding water for injection, stirring to mix uniformly, adding sodium hydroxide to dissolve the lansoprazole and the disodium ethylenediaminetetraacetate, and adjusting the pH value to 11.5-12.0; (2) rubber plug processing; (3) aseptic filtration and subpackage; and (4) vacuum freezing and drying. For lansoprazole medicaments which are very easy to react with effusion from the rubber plug, the lansoprazole composition for injection, provided by the invention, can simultaneously and effectively ensure that visible foreign matters and insoluble particles of products conform to the requirement of an injection. The invention remarkably improves the quality of products, avoids hidden dangers brought to the clinical medication safety of patients due to the unqualified visible foreign matters and insoluble particles, and achieves a better curative effect and a lower clinical adverse reaction rate.
US20070299105 2-Cyanopropanoic Acid Amide and Ester Derivatives and Methods of Their Use This invention provides compounds of formula I or a pharmaceutically acceptable salt thereof that are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatoid arthritis.
US20110230556 Diglycidic Ether Derivative Therapeutics and Methods for Their Use This invention provides compound having a structure of Formula I or Formula II. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.
CA2545962A1 Use of organic buffering agents to enhance the antimicrobial activity of pharmaceutical compositions The use of organic buffers to enhance the antimicrobial activity of aqueous pharmaceutical compositions is described. The buffers have tri-hydroxy functional groups and terminal acid groups, and are zwitterionic at physiological pH conditions. The most preferred buffer is tricine. The invention is particularly directed to the use of tricine to enhance the antimicrobial activity of ophthalmic compositions, such as solutions for disinfecting contact lenses and artificial tear compositions.
US20120220548 Compositions and methods for treatment of virus-associated cancer cells Compositions, methods and kits are provided for treating a cancer, tumor or pre-cancerous tissue condition resistant to a chemotherapeutic agent, the tissue condition having one or more proteins or tumorigenesis markers induced by, upregulated by or otherwise associated with virus exposure. A marker may be a receptor for, or may operatively regulate production or use of hyuronan, for example by mediating a hyaluronan-associated signal path or affecting expression of a protein or signaling pathway of the diseased tissue. A treatment composition includes a competitor of hyaluronan interactions and further includes or is co-administered with a drug, e.g., a chemotherapy agent to which the virus-associated condition would be resistant absent the hyaluronan or competitor.
US7084107 Methods for stabilizing liquid nutritional products and products so stabilized Nutritional solutions and methods of making same are disclosed. The solutions include protein, lipid, and a carbohydrate source including high amylose starch and guar gum.
CN103565826A High-density compound calcium carbonate The invention relates to high-density compound calcium carbonate. The high-density compound calcium carbonate is prepared from 88-90% of calcium carbonate powder, 6-8% of pregelatinized starch, 3-4% of white dextrin, and 0.6-0.8% of magnesium stearate. The product which is finally prepared by selecting materials for calcium carbonate powder, and mixing and pelletizing the calcium carbonate powder, the pregelatinized starch, the white dextrin and the magnesium stearate in a mixing pelletizer has concentrated particles, and is good in flowing property, and good in compressibility; the uniformity of tablet weight at the tabletting stage is facilitated; the sizes of the tablets under equal conditions are reduced; meanwhile, the loss of a machine mold can be reduced; the service life is prolonged. Thus, the quality of the product is improved, and the cost is reduced.
CN101815513B Ophthalmic formulation containing paracetamol A new use for paracetamol in a method of treating glaucoma, which method comprises administering to a patient in need of such treatment 500 mg to 1000 mg of paracetamol in oral format 4 to 6 hourly. An ophthalmic solution is also provided containing between 0.1 to 5% of paracetamol which is administered as one to two drops in each eye 4 to 6 hourly. The ophthalmic solution further includes one ormore of the following excipients: hydroxypropylmethylcellulose, benzalconium chloride, polyacrylic acid such as Teargel TM.
EP0765357B1 Antiviral dendrimers An antiviral compound comprises a dendrimer such as a polyamidoamine or polylysine dendrimer having a plurality of terminal groups, wherein at least one of the terminal groups has an anionic- or cationic-containing moiety bonded thereto, particularly a sulfonic acid-containing, carboxylic acid-containing or trimethylammonium-containing moiety or the like.
US20110212169 METHOD FOR PRODUCING POWDER CONTAINING NANOPARTICULATED SPARINGLY SOLUBLE DRUG, POWDER PRODUCED THEREBY AND PHARMACEUTICAL COMPOSITION CONTAINING SAME (As Amended) Disclosed are a method for preparing a powder containing a nanoparticulated sparingly soluble drug, a powder prepared thereby, and a pharmaceutical composition containing the same. The disclosed method includes: providing a uniformly dispersed solution of a sparingly soluble drug which is formed into nanoparticles in the presence of a surface stabilizer; mixing the uniformly dispersed solution with a water-soluble dispersant solution; and drying the mixed solution to obtain the powder. When the powder containing the nanoparticulated sparingly soluble drug obtained by the disclosed method is redispersed in an aqueous solution, the sparingly soluble drug retains a particle size in the nano scale while the solubility and the dissolution rate of the drug are increased, thereby providing enhanced bioavailability. Consequently, the present disclosure can be useful in the development of preparations of a sparingly soluble drug for oral or parenteral administration.
US7026475 carbapenem derivatives with an antibacterial activity Compounds of formula (I) wherein R1, R2, R3, R4, R5, n, and m, are as defined herein, or an enantiomer or diastereomer thereof, or a pharmacologically acceptable salt thereof, processes for preparing these compounds, and their use in pharmaceutical compositions.
EP1967517A1 Probe for diagnosis of conformational disease The invention provides a probe compound useful for early diagnosis of conformation disease, a composition and a kit comprising it for diagnosis for conformation disease, and a medical composition for treatment and/or prevention of conformation disease.
CN102018724A Preparation method of medical artificial cerebrospinal fluid and application thereof The invention provides a preparation method of medical artificial cerebrospinal fluid and an application thereof, belonging to the fields of medical treatment and public health. The technical scheme of the invention is that: firstly, preparation prescription of the artificial cerebrospinal fluid includes 6.279g of sodium chloride, 0.216g of potassium chloride, 0.353g of calcium chloride, 0.488g of magnesium chloride, 1.932g of sodium bicarbonate, 0.6g of glucose, 0.358g of disodium hydrogen phosphate and 1000ml of distilled water; secondly, the preparation method includes the following steps: 1, disinfection; 2, thinner preparation; 3, artificial cerebrospinal fluid preparartion; and 4, storing; thirdly, application range includes the following diseases or conditions: (1) cleaning of craniocerebral injury and war wound dirt; (2) subarachnoid hemorrhage; (3) cerebral hemorrhage broken into the ventricle; (4) central nervous system infectious diseases; (5) cerebrospinal fluid fistula; and (6) washing of brain wound in brain operation.
CN101703477A Coenzyme Q10 mini-pill and preparation method thereof The invention provides a mini-pill preparation of coenzyme Q10, which is prepared by the coenzyme Q10 and medicinal auxiliary materials. The mini-pill preparation is characterized in that the medicinal auxiliary materials are an excipient and a binding agent, wherein the mini-pill preparation comprises the following ingredients in percentage by weight: 2 percent to 80 percent of the coenzyme Q10, 12 percent to 97 percent of the excipient and 1 percent to 8 percent of the binding agent. The mini-pill preparation can be prepared into a slow-release or an enteric preparation according to requirements. The mini-pill preparation of the coenzyme Q10 has high dissolution rate and high bioavailability, and the method is simple and convenient and easy to operate.
EP1871742A1 Preparation of ý2-methyl-5-phenyl-3-(piperazin-1-ylmethyl)¨pyrrole derivatives A process for the preparation of compounds of Formula (I) and their pharmaceutically acceptable acid addition salt wherein R1 is phenyl or substituted phenyl, R3 is selected from a group of formula (a), n = 0-2 and X = -NCH3, CH2, S, SO, or SO2 wherein R2 and R5 are as defined herein.
US7195787 Topical cosmetic Topical cosmetic compositions for application to the skin comprises a suitable diluent or carrier in combination with a synergistic mixture of three anti-free-radical agents selected from ascorbic acid, its salts, esters, glucosides and glucosamines; tocopherol and its esters; herbal extracts selected from gingko biloba, morus alba, origanum vulgare, panax ginseng, rosmarinus officinalis, birch extract, camellia sinensis, acerola cherry powder and grape seed oil.
CN102106883A Medicinal composition containing asiaticoside and tretinoin A medicinal composition for treating acne and cicatrix contains asiaticoside and tretinoin medicaments, and comprises preparation for external use and preparation for oral use. Proved by experiments, the medicinal composition disclosed by the invention has remarkable efficacies in inhibiting bacterial related to the acne, resisting inflammation, reducing the thickness of stratum corneum and treating the cicatrix or cicatrixc hyperplasia caused by the acene and good safety.
WO2013186320A1 Pharmaceutical composition comprising crystalline posaconazole The present invention relates to a pharmaceutical composition which comprises crystalline posaconazole and one or more non-ionic surfactants, wherein at least one non-ionic surfactant is an ethoxylated hydrogenated castor oil.
US20090221522 Methods to correct gene set expression profiles to drug sensitivity The present invention comprises a treatment approach based on gene set-expression signatures that systematically connects a sample to a profile from a reference database to extrapolate the most effective therapeutic agent. Further disclosed are methods to optimize combination treatments.
US20100160426 Crystalline genistein sodium salt dihydrate The disclosure relates to a new crystalline form of genistein. The disclosed crystalline form is crystalline genistein sodium salt dihydrate. The disclosure also relates to the novel genistein salt composition represented by this crystalline form. Therapeutic compositions containing crystalline genistein sodium salt and a pharmaceutically acceptable carrier are described. The disclosure also relates to therapeutic methods comprising the step of administering to a patient in need thereof a therapeutically effective amount of a therapeutic composition containing the crystalline form of the disclosure or crystalline genistein sodium salt dihydrate.
US7521461 2-{[4-(2-Oxo-2-{[4-(trifluoromethyl)benzyl]amino)ethyl)phenoxy]methyl}benzoic acid; peroxisome proliferator activated receptors alpha and gamma agonist; antidiabetic agents; Insulin Resistance Syndrome (IRS); cardiovascular disorders; myocardial infarction; stroke; atherosclerosis; dyslipidemia A compound of formula (I) wherein R1 represents aryl optionally substituted by a heterocyclic group or a heterocyclic group optionally substituted by aryl wherein each aryl or heterocyclic group is optionally substituted; the group —(CH2)m-T-(CH2)n—U—(CH2) p— is attached at either the 3 or 4 position in the phenyl ring as indicated by the numbers in formula (I) and represents a group selected from one or more of the following: O(CH2)2, O(CH2)3, NC(O)NR4(CH2)2, CH2S(O2)NR5(CH2)2, CH2N(R6)C(O)CH2, (CH2)2N(R6)C(O)(CH2)2, C(O)NR7CH2, C(O)NR7(CH2)2, and CH2N(R6)C(O)CH2O; V represents O, S, NR8 or a single bond; q represents 1, 2, or 3; W represents O, S, N(R9)C(O), NR10, or a single bond; R2 represents halo, a C1-4 alkyl group which is optionally substituted by one or more fluoro, a C1-4 alkoxy group which is optionally substituted by one or more fluoro, a C1-4 acyl group, aryl, an aryl C1-4 alkyl group, CN or NO2; r represents 0, 1, 2 or 3; R3 halo, a C1-4 alkyl group which is optionally substutited by one or more fluoro, a C1-4 alkoxy group which is optionally substituted by one or more fluoro, a C1-4 acyl group, aryl, an aryl C1-4 alkyl group, or CN; s represents 0, 1, 2 or 3; and R4, R5, R6, R7, R8, R9, and R10 independently represent H, a C1-10 alkyl group, aryl or an aryl C1-4 alkyl group or when m is O and T represents a group N(R6)C(O) or a group (R5)NS(O2) then R1 and R6 or R1 and R5 together with the nitrogen atom to which they are attached represent a heteroaryl group; with provisos and pharmaceutically acceptable salts thereof, processes for preparing such compounds, their utility in treating clinical conditions associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.
US8710000 Insulin derivative The present invention relates to novel human insulin derivatives which are soluble at physiological pH values and have a prolonged profile of action. The invention also relates to pharmaceutical compositions containing such derivatives and to methods of treating diabetes and hyperglycaemia using the insulin derivatives of the invention.
CN101597311A Erythromycin derivative and application thereof The invention belongs to the technical field of medicine, which relates to an erythromycin derivative. The structure of the erythromycin derivative is shown as (I): in the right structural formula (I), a and e can be selected from 0 and 1, b, c and d can be selected from 0, 1, 2 and 3, but a, b, c, d and e can not be 0 simultaneously. The invention also provides innoxious salt and a hydrated substance thereof which are formed by the derivative shown in the structural formula and are acceptable in pharmacy. The derivative has better tumour-suppressing activity, and can be used for the application of a tumour cell propagation suppressor in the aspect of preparing anti-tumour medicines.
CN1857205A Slow released injection containing blood vessel inhibitor and its synergist The slow released injection containing blood vessel inhibitor and its synergist consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is blood vessel inhibitor carboxyl amino triazole, Irotinat, Lapatinat, etc and/or blood vessel inhibitor synergist selected from toporase inhibitor and tetrazin compound. The slow releasing supplementary material is one of difatty acid-sebacic acid copolymer, poly(erucic acid dipolymer-sebacic acid), poly(fumaric acid-sebacic acid), polylactic acid, etc or their composition. The suspending agent is carboxymethyl cellulose, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for improving the treating effect of chemotherapeutic and/or radiotherapeutic medicine.
WO2007083146A3 The treatment of cognitive and psychotic disorders An anti-diabetic agent such as insulin is useful for the treatment of a psychotic disorder such as a schizophrenic disorder.
CN101234087A Poside containing anti-cancer sustained-release injection The invention relates to anticancer sustained release injection which comprises sustained release microspheres and menstruum, wherein, the sustained release microspheres comprise anticancer active components and sustained release auxiliary material; the menstruum is special menstruum that contains suspending agent. The anticancer active components are fotemustine, nimustine, carmustine or combination of bendamustine and mitozolomide, docetaxel, etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluorouracil or mitomycin C; the sustained release auxiliary material is polylactic acid and polylactic acid copolymer, polyethylene glycol and polylactic acid copolymer of polyethylene glycol, terminal carboxyl group polylactic acid copolymer, EVAc, fatty acid and decanedioic acid copolymer, etc.; viscosity of the suspending agent is 100cp-3,000cp (at 25 DEG C-30 DEG C), and the suspending agent is selected from sodium carboxymethylcellulose, etc. The sustained release microspheres can also be made into sustained release implant; the injection or implant is injected or placed in or around tumor so as to reduce general reaction of the drug and selectively improve and keep local concentration for about 30-50 days. The anticancer sustained release injection can be used solely and can also promote anti-tumor effects of non-operative treatments, such as chemotherapy and/or radiotherapy, etc.
WO2014068516A3 A method of managing urolithiasis and related urological disorders The present disclosure relates to a method of managing urolithiasis or related urological disorders in a subject in need thereof, using pharmaceutical composition comprising trigonelline or its derivative(s) and 4-hydroxyisoleucine or its derivative(s), optionally along with excipient(s).
EP2310031B1 Combination of a tiliroside and lysine-valine 5 diaminohydroxybutyrate The invention relates to a combination including at least one bioflavonoid, in particular tiliroside, and at least one peptide, in particular palmitoyl Lysine-Valine-5 diaminohydroxybutyrate. The invention also relates to a cosmetic or dermatological composition containing said combination.
CN1768812A Medicinal composition for removing dampness to relieve itching and its preparation method and uses The invention relates to a pharmaceutical composition for removing dampness and relieving itching, and process for preparation, wherein the composition is prepared from cnidium fruit, goldthread root, corktree bark, Chinese dittany bark, flavescent sophora root, giant knotweed rhizome, Philippine violet herb, broom cypress fruit, knotgrass, oriental wormwood, atractylodes rhizome, pricklyash peel, borneo camphor, and can be made into the dosage forms of lotions, electuary, filming agent, liniment, suppository, aerosol, spray, externally-used tablet or effervescent tablet.
CN102746363A High purity aescine B bulk drug, its preparation method and medical application Belonging to the field of medicinal technologies, the invention particularly relates to a high purity aescine B bulk drug, its preparation method and application as anti-inflammatory exudation and edema bulk drugs. The bulk drug provided in the invention has the advantages of simple preparation process, environmental protection, controllable quality, stronger activity than existing aescine drugs, good safety, and good application prospects.
WO2014001353A1 Pharmaceutical compositions and treatment of mastitis The present invention relates to a pharmaceutical composition and methods of treating and/or preventing mastitis in non-human mammals. More particularly, the present invention relates to the treatment of mastitis in cows. The pharmaceutical composition comprises a mixture of a phosphonic acid and at least one antimicrobial.
US20070043105 Preventive for cerebal stroke recurrence The invention provides a novel cerebral stroke recurrence inhibitor, and relates to a simple evaluation method for an cerebral stroke recurrence inhibitor. According to the simple evaluation method using stroke-prone spontaneously hypertensive (SHR-SP) rats, which has been established by the present inventors, it has been confirmed that atorvastatin is effective for preventing cerebral stroke recurrence, for relieving cerebral stroke recurrence-accompanied neurologic symptoms, and for improving survival rate after onset of the stroke. Accordingly, atorvastatin is useful as an cerebral stroke recurrence inhibitor.
WO2012145254A2 Methods of using inhibitors of rorϒt to treat disease Ursolic acid ("UA") and analogs of UA are taught as RORϒt inhibitors useful in the treatment of a diseases or conditions ameliorated by the expression or production of IL-17, IL-17F, IL-21, and IL-22, and the differentiation and/or development of TH17 cells.
CN101374845A Novel compounds and use thereof A compound of formula (I) wherein R<1> is selected from H, F, Cl, Br, CF3, C1-C6 alkoxy and OH; R<2> is selected from H and C1-C6 alkyl; n is 1-12; m is O or 1; Y is selected from CH2, NR<3>, (NR<3>R<4>)+X'', O and S; R<3> and R<4> are independently selected from H and C1-C4 alkyl; and X'' is selected from pharmaceutically acceptable anions. A method of preparing the compound, its use as a pharmaceutical, and a method of treatment.
CN102766165A Methods for synthesizing molybdopterin precursor z derivatives Provided herein are synthetic methods for preparing a compound of formula (I): Also provided herein are synthetic methods for preparing a compound of formula (XIII): The disclosure also provides useful intermediates, derivatives, prodrugs, and pharmaceutically acceptable salts, solvates and hydrates of the formula (I) and formula (XIII) compounds. These compounds are useful for treating diseases associated with molybdenum cofactor deficiency.
CN103463063A Application of Lycojaponicumin C in preparation of medicines for treating laryngeal cancer The invention discloses an application of Lycojaponicumin C in preparation of medicines for treating laryngeal cancer, belonging to the technical field of new applications of medicines. The evaluation on an in vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anti-tumor activity shows that the Lycojaponicumin C also has an obvious inhibiting effect on the growth of human laryngeal cancer cell lines HEP-2, TU686, M2e and M4e. Therefore, the Lycojaponicumin C can be used for the preparation of the medicines for treating the laryngeal cancer and has good development and application prospects. The application of the Lycojaponicumin C in the preparation of the medicines for treating the laryngeal cancer is disclosed for the first time. As the skeleton type of the Lycojaponicumin C belongs to a brand-new skeleton type, the Lycojaponicumin C has unexpected strong inhibitory activity on laryngeal cancer cells.
CN101919836A New application of rosmarinic acid The invention relates to a new application of rosmarinic acid, and provides an application of rosmarinic acid in preparing a medicine for treating or preventing hepatitis, in particular to an application of rosmarinic acid in preparing a medicine for treating or preventing hepatitis b and hepatitis c. The rosmarinic acid has obvious inhibiting effects on HBsAg and HbeAg, and has obvious inhibition ratio on HCV virus.
CN101961319A Silybin meglumine enteric agent with high bioavailability and preparation method thereof The invention relates to the field of medical agent, in particular to a silybin meglumine enteric agent with high bioavailability and a preparation method thereof. The preparation method is characterized by comprising the following steps of: preparing the silybin meglumine into solid dispersoid; adding the medical auxiliary materials to prepare to be the grain, the tablet or the pellet; and packing the grain, the tablet or the pellet into an enteric coat. With the unique shape, the silybin meglumine can not be released in the stomach but can be fast dissolved and absorbed in the intestinal canal; and by being prepared to be the solid dispersoid, the silybin meglumine increases the solubility in the water. Therefore, the invention increases the absorbed dose of the silybin meglumine, has higher bioavailability compared with the common tablet or capsule, is good for curing the hepatopathy, and is simple in preparation technology.
EP1581224A1 Tiotropium-containing medicament combinations used for inhaling The invention relates to novel medicaments used for inhaling, comprising one or several, preferably one, tiotropium salt in combination with one or several pharmaceutically acceptable acid addition salts of a compound of formula 2', wherein radicals R1, R2, R3, and R4 can have the meanings indicated in the description and in the claims. Also disclosed are methods for the production thereof and the use thereof in the therapy of respiratory diseases.
EP2303336A2 Sulfonylurea receptor and means for treating ischaemia We disclose agents useful in the treatment of diseases or conditions that would benefit from improved muscle function and including pharmaceutical compositions and diagnostic tests for determining the predisposition of a subject, in particular a male subject, to cardiovascular disease.
WO2010100144A1 Fused bicyclic compounds as inhibitors for pi3 kinase The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.
EP0977767B1 Aminooxy-modified oligonucleotides Nucleotide compositions containing aminooxy moieties are provided. In accordance with preferred embodiments, oligonucleotides and oligonucleotide analogs are provided which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligonucleotide is modified to include an aminooxy moiety.
EP2222650A1 Substituted pyrazinyl amide compounds as modulators of the histamine h3 receptor Certain substituted pyrazinyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
WO2014036548A1 Macromolecular prodrugs for hard tissue and methods of use thereof Compositions for intravenous administration and methods for treating bone diseases, disorders, and fractures comprising macromolecular prodrugs of hydrophobic bone anabolic agents are provided. Specifically, novel macromolecular amphiphilic prodrugs wherein at least three molecules of simvastatin are conjugated to polyethylene glycol, which spontaneously form micelles in aqueous solutions are provided.
US20050095297 Nanoparticulate formulations of fenofibrate Nanoparticles and nanoparticle formulations or suspensions are provided which comprise a fibrate and vitamin E TPGS. The nanoparticles may have a mean diameter, measured by photon correlation spectroscopy, in the range of from about 100 nm to about 900 nm. Pharmaceutical formulations and uses of such compositions are also provided.
CN103655790A Natural pharmaceutical composition, and preparation method thereof The invention relates to a natural pharmaceutical composition, and a preparation thereof. The natural pharmaceutical composition is composed of rhizoma coptidis and hawthorn water decocted concentrated extract, berberine, and hawthorn general flavone at a ratio of 2-8:1-4:3-8. The natural pharmaceutical composition possesses excellent curative effect on cancer chemotherapy related diarrhea.
CN102949413A Method for preparing invert sugar and electrolytes injection The invention belongs to the field of medical technologies, and mainly relates to a method for preparing an invert sugar and electrolytes injection. Specifically, the method disclosed by the invention improves the stability and safety of compatibility from the process source, and the invert sugar and electrolytes injection prepared by using the method disclosed by the invention can be safely compatible with 70 kinds of commonly used clinical medicines such as cefodizime sodium, thereby improving the safety, applicability and convenience of clinical medications.
WO2013071400A8 Apocynin-lipoic acid conjugates and uses thereof cross-reference to related applications The present application relates to novel apocynin-lipoic acid covalent conjugates, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions that are mediated by oxidative stress. In particular, the present application includes compounds of Formula (I), and compositions and uses thereof.
US20110124552 GMCSF and Truncated CCL2 Conjugates and Methods and Uses Thereof A conjugate protein comprising a GM-CSF or a fragment thereof and a truncated CCL2 is described. The conjugate protein has unexpected immune suppressive, anti-obesity and tumoricidal properties and is useful in a variety of therapeutic applications.
WO2012069917A1 Bicyclic gpr119 modulators The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR1 19 receptor by using either alone or in combinations of Formula (I).
CN101579442A Pharmaceutical composition for lowering blood sugar and blood fat A pharmaceutical composition for lowering blood sugar and blood fat is disclosed, which comprises cortex lycii radicis, vitamin A, beta-carotene, vitamin B complex, vitamin C, vitamin D, vitamin E, macroelements including calcium, potassium and magnesium, and microelements including zinc, selenium, ferrum, chrome, copper, molybdenum, iodine and manganese, and which is mainly suitable for people having high blood sugar and blood fat, is highly effective to lower blood sugar and blood fat and can be used for a long term or according to the course of treatment.
CN102743409A Application of poly mannuronic acid propyl ester sulfate in preparing anti- H1N1 influenza A virus medication The invention provides applications of poly mannuronic acid propyl ester sulfate (PMS) in preparing anti- H1N1 influenza A virus medication. Experiments of the invention prove that PMS not only has great inhibition effect on the neuraminidase of the influenza A virus, but also has relatively good protection effect on canine kidney epithelial cells infected with the H1N1 influenza A virus, and can reduce the replication of the H1N1 virus with an effect that equal to the positive control medication ribavirin. Additionally, the PMS can effectively reduce the death rate of mice infected with the H1N1 influenza A virus and the survival time of the mice are prolonged. The poly mannuronic acid propyl ester sulfate provided by the invention has significant activity of inhibiting the neuraminidase of the H1N1 influenza A virus, and is proved to have good anti- H1N1 influenza A virus activity both in vivo and in vitro experiments, which shows the wide application prospect of the poly mannuronic acid propyl ester sulfate in preparing anti-H1N1 influenza A virus medication.
CN102000039A Stable iloperidone capsule medicament composite The invention discloses a stable iloperidone capsule medicament composite and a preparation method thereof. The invention is characterized in that the formula for preparing 1000 grains of the capsules comprises the following components: 1g-6g of iloperidone, 40g-240g of lactobiose (Megglec80), 10g-60g of microcrystalline cellulose (JRS12), 5g-30g of croscarmellose sodium and 0.2g-1.2g of magnesium stearate. The invention also relates to a preparation method of the iloperidone capsule medicament composite, which comprises the following steps of: drying raw materials and auxiliary materials at 80 DEG C for 3 hours; uniformly mixing the components according to the equal proportion; filling capsules and obtaining the iloperidone capsule medicament composite. The iloperidone capsule prepared by the prescription and the preparation method has the advantages of good flowability, good dissolution, small filling volume difference, high biology utilization degree and good curative effect.
CN102793671A Human recombinant epidermal growth factor (hrEGF)-modified cisplatin-loaded polymeric nanoparticles and preparation method and application thereof The invention relates to the technical field of medicines, in particular to human recombinant epidermal growth factor (hrEGF)-modified cisplatin-loaded polymeric nanoparticles and a preparation method and application thereof. The hrEGF-modified cisplatin-loaded methoxy polyethylene glycol-polylactic-co-glycolic acid-polylysine (mPEG-PLGA-PLL) nanoparticles are obtained by preparing cisplatin-loaded nanoparticles by taking mPEG-PLGA-PLL as a carrier by an ultrasonic emulsification/solvent evaporation method, and then connecting an amino-terminated group and a hrEGF. The nanoparticles can be specifically combined with epidermal growth factor receptors (EGFR) of the surfaces of tumor cells, and the endocytosis is performed, so that the toxic or side effect of cisplatin is reduced, and the aims of reducing poisonousness and synergizing are fulfilled. The nanoparticles can be used for the preparation of anti-tumor medicines; and particularly, the treatment research of ovarian cancer proves that the nanoparticles have high targeting, have a strong killing effect, and have a good application prospect in the chemotherapy of ovarian cancer.
US20130004425 Biomineral and Metal Binding Liposomes, Their Synthesis, and Methods of Use Thereof Drug carriers, methods of synthesizing, and methods of use thereof are provided.
US20060252780 Fused pyrimidine derivatives A fused pyrimidine derivative is presented. The derivatie has an insulin secretion stimulating activity represented by Formula (I): {wherein R1 represents a hydrogen atom, lower alkyl, or the like; n represents an integer of 0 to 3; and X1 and X2 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like; and formula (II): represents formula (III): [wherein X—Y—Z represents R2C═CR3—NR4 (wherein R2, R3 and R4 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like)]}, or a pharmaceutically acceptable salt thereof.
CN103539731A Pyridine-2-amide compound as well as preparation method, pharmaceutical composition and use thereof The invention relates to a pyridine-2-amide compound shown as a general formula I as well as a preparation method, a pharmaceutical composition and use thereof. The compound as an integrase inhibitor is used for preparing medicines for treating diseases mediated by various vetrovirus integrases including HIV-1 (Human Immunodeficiency Virus-1) integrase.
WO2008152226A3 Homogeneous and stable composition rich in oleaginous substances based on a milk product, method for the preparation thereof and uses thereof The present invention relates to a stable and homogeneous milk composition based on milk comprising at least one cyclodextrin and at least one oleaginous substance. It also relates to the preparation thereof and also to products prepared therefrom, such as food compositions, powders, medicinal food products, and nutraceutical, cosmetic, pharmaceutical and veterinary compositions.
CA2167578C Chicken anemia virus mutants and vaccines and uses based on the viral proteins vp1, vp2 and vp3 or sequences of that virus coding therefor Novel proteins of the Chicken Anemia Virus are described and compositions for preventing or treating infections with that virus (CAV), in particular vaccines less pathogenic than the CAV itself, but yet leading to neutralizing antibodies in the immunized animal. Besides, there are described compositions containing antibodies against parts of the CAV for the control of infections with CAV and anti-idiotype antibodies. The invention also provides antibodies and test kits for the detection of CAV.Recombinant DNA molecules derived from CAV and host cells transfected therewith and vaccines based on these host cells are made possible by this invention. The invention also comprises living virus vaccines in which a piece of DNA is brought into a virus infectious to the host. Besides, the invention provides uses of proteins of CAV in the induction of apoptosis, in particular in tumor cells. It further provides the induction of cell death by means of gene therapy.
EP1970059A1 Medication with Dobesilat-Calcium for treatment and prophylaxis of tendon disease Treating and/or preventing tendon diseases in patient, involves administering composition comprising calcium dobesilate (2,5-dihydroxybenzosulfonate) to the patient.
WO2009060186A1 Sulfonated precursors of thymidine for the treatment of epithelial hyperplasias This invention relates to pharmaceutical compositions comprising a sulfonated biological precursor of thymidine, such as a precursor of 4-thiothymidine (4-TT), and their use in the photodynamic treatment of skin hyperplasias, including cancer, psoriasis, actinic keratosis and keloids, by topical or systemic administration.
US20090264454 Combined hydrocodone and analgesic formulation and method The present invention is directed to co-administration of hydrocodone and a second analgesic agent for the treatment of pain. A pharmaceutical composition suitable for the co-administration contains a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of at least one second analgesic agent. A ratio of the hydrocodone or pharmaceutically acceptable salt thereof to the at least one second analgesic agent in the composition is within a range that provides greater pain relief than that obtainable by the administration of the hydrocodone or second analgesic agent alone. Examples of pharmaceutical compositions for co-administration of the agents are those containing hydrocodone and indomethacin (“Indocodone”), hydrocodone and naproxen (“Naprocodone”), hydrocodone and diclofenac (“Diclodone”) and hydrocodone and tramadol (“Tramacodone”).
US20090061031 Compositions and methods for treating obesity, obesity related disorders and for inhibiting the infectivity of human immunodeficiency virus The present invention relates to methods and pharmaceutical compositions for treating obesity or obesity-related disorders in a subject suffering from or predisposed to developing obesity or an obesity-related disorder, or for inhibiting the infectivity of HIV, by administering oleuropein, an analogue or derivative thereof, or the major metabolites of oleuropein including oleuropein aglycone, hydroxytyrosol, and elenolic acid or their analogues, or derivatives thereof, an iridoid glycoside, or a secoiridoid glycoside or analogues or derivatives thereof, or any combination of the foregoing including olive leave extract. The invention also relates to methods for screening/diagnosing a subject having, or predisposed to having obesity or a related disorder by measuring the expression profiles of an adipogenic gene selected from PPARγ2, LPL and αP2 gene and gene product, or other adipogenic, lipogenic, or lipolytic genes and gene products in an individual. The invention further provides for screening for novel oleuropein analogues.
US20060035874 Pharmaceutical products and composition comprising specific anticholinergic agents, beta-2 agonists and corticosteroids This invention relates to pharmaceutical products and compositions for use in the treatment of asthma and related disorders, and especially but not exclusively for the treatment of chronic obstructive pulmonary disease (COPD). More particularly, the invention provides pharmaceutical products and compositions comprising specific anticholinergic agents, β-2 agonists and corticosteroids.
CN1830438A Preparation method of vitamin C freeze dried powder injection A freeze-dried powder injection of VC for preventing and treating scurvy, acute and chronic infectious diseases, purpura, Keshan disease, etc is prepared from VC, sodium hydrogen sulfate, and disodium versenate through ultrasonic treating, adding CO2 saturated water for injection in dark condition and N2 atmosphere, regulating pH value and temp, etc.
CN103058994A Urea derivative and medicinal application thereof The invention relates to N-(4-((4-(3-(3-tert-butyl-1-p-methylphenyl-1H-pyrazole-5-yl) ureido) naphthalene-1-base oxygen) methyl) pyridine-2-yl)-2-methoxy acetamide and fumarate of a derivative thereof or a solvate thereof acceptable in pharmacology and an application for preparing a medicine for treating and/or relieving and/or preventing influenza.
CN1985805A Lung targeting clarithromycin microsphere for animal and birds and its preparing method The present invention belongs to the field of veterinary medicine technology, and is especially lung targeting clarithromycin microsphere for animal and its preparation process. The clarithromycin microsphere is prepared with clarithromycin as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving clarithromycin in gelatin solution and adding Span-80 and liquid paraffin through stirring to obtain emulsion; cooling in icy bath to below 5 deg.c and adding glutaraldehyde through stirring for cross-linking and curing; dewatering with isopropyl alcohol and suction filtering; washing with isopropyl alcohol and ethyl ether to eliminate glutaraldehyd, washing with petroleum ether to eliminate liquid paraffin in the surface of microsphere and vacuum drying at room temperature to obtain clarithromycin microsphere. The medicine has raised tissue selectivity, delayed release, raised curative effect and lowered toxic side effect.
CN101580530A Amino acid conjugate prodrug of pentacyclic triterpenoid and medical application thereof The invention provides a conjugate formed by pentacyclic triterpenoid and amino acid through an ester bond or an urethane bond of the formula I and the formula II, wherein R1 is hydrogen, a methyl, an isopropyl, an isobutyl, a 2-methylpropyl or a benzyl; X is H2 or O; R2 is H, CH3 or COOH; R3 is CH3 or COOH; and R4 is H or CH3.
US20100316677 Use of bamboo leaf total flavones in the preparation of medicine and health food for prevention and treatment of prostatic diseases This invention discloses the new uses of Lophatherum Total Flavones in medical, pharmaceutical, and healthcare fields. Lophatherum Total Flavones have effects of anti-bacteria, inhibiting bacteria, anti-inflammation, anti-prostatic hyperplasia, anti-platelet aggregation, anti-tumor, and promotion of immunity, etc., with safety and without toxicity, suitable for chronic oral administration, and especially suitable for prevention and treatment of senile chronic degenerative diseases; Lophatherum Total Flavones may be used in fields of pharmaceutical and foods, as a natural drug for prevention and treatment of prostatitis, prostatic hyperplasia, and prostate cancer, or as a dietary supplement.
US20060252769 Obesity, type 2 diabetes, sleep disorders, ischaemic or haemorrhagic strokes, antiemetic; toxicity; side effect reduction; 2-((benzofuran-4-yl)carbonylaminomethyl)-1-((4-(5-(4-fluorophenyl)-2-methyl)thiazolyl)carbonyl)-4-methylpiperazine This invention relates to piperazine bis-amide derivatives and their use as pharmaceuticals.
EP1370259B1 Use of melatonin in the manufacture of a medicament for treating attention deficit hyperactive disorder The present invention relates to the use of at least one of melatonin, a melatonin analogue, or a pharmaceutically acceptable salt thereof in the treatment of attention deficit hyperactive disorder (ADHD). Melatonin or its analogue may be used alone or in combination with one or more other active ingredients, and is preferably formulated as a composition for controlled release.
CN103588769A Synthesis of novel dihydrogen pyrazole-thiazolinone derivatives and application of dihydrogen pyrazole-thiazolinone derivatives in anticancer drugs Dihydrogen pyrazole-thiazolinone derivatives are characterized by having the following general formula as described in the specification, wherein in the structural formula, R1 is 2-pyridine ring, 3-pyridine ring, or 4-pyridine ring, and R2 is hydrogen, chlorine, bromine, fluorine, methyl, or methoxyl. The invention discloses a preparation method for the dihydrogen pyrazole-thiazolinone derivatives and inhibition effects of the dihydrogen pyrazole-thiazolinone derivatives on human breast cancer cell lines (MCF-7), proliferation epidermal carcinoma cells (Hela), and mouse melanoma cells (B16-F10), so the dihydrogen pyrazole-thiazolinone derivatives can be applied in preparation of antitumor drugs.
WO2012034091A1 Imidazo [1, 2] pyridazin compounds and compositions as trk inhibitors The invention provides compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.
CN101579518A Granules and powdered medicine for preventing and treating vomiting The invention discloses a preparation method of granules and powdered medicine for preventing and treating vomiting. The preparation method comprises the following steps of: first mixing terra frava usta, ruddle, raw radix paeoniae alba, clear tuber pinellia, codonopsis affinis, Chinese gentian, indigo naturalis, evodia rutaecarpa, Guizhou ginger, hawthorn and malt; adding 8 times water and 6 times water for decoction and extraction for twice and respectively for 2 hours; merging and then concentrating the extraction liquid; and drying to prepare a dry paste; merging the dry pastes obtained from twice preparations, then cogrinding into fine powder; adding soda powder, powdered milk, sucrose, dextrine, flavoring essence, powdered oil and protein honey; and after mixing, adding starch as accessorial ingredient to prepare the granules or prepare the powdered medicine, thus obtaining the granules and powdered medicine after bagging.
CN102000099A Medicine for treating breast cancer and preparation method thereof The invention discloses a medicine for treating breast cancer and a preparation method thereof. The medicine is prepared from effective medicinal components and medicinal adjuvant in proportion by weight, wherein the effective medicinal components comprise 3 beta-oxygen-alpha-L arabopyranose-28-norursol-12, 17-diene, and the effective medicinal components have a structural formula. The preparation method comprises the following steps of: 1. pulverizing charred sanguisorbae radix as a medicinal raw material, repeatedly extracting the medicinal raw material, and filtering to obtain a liquid extract; 2. dispersing the liquid extract obtained in step 1 with water, extracting with chloroform, and recovering solvent in the extract liquor to obtain an extract; 3. separating the extract obtained in step 2 by gel column chromatography, and leaching the obtained solid recrystal to obtain compound effective medicinal components; and 4. weighing 20-90% of effective medicinal component by weight ratios and other pharmaceutic adjuvants to prepare the medicine. The medicine has good effect on treating breast cancer, and can substitute for oral western medicines taken in duration of chemotherapy after an operation.
CA2688823A1 Heterocyclic kinase modulators The present disclosure provides heterocyclic protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.
EP1290182B1 Sphingosine kinase and uses thereof The present invention relates generally to a method of modulating the growth of cells and, more particularly, to a method of down-regulating the growth of neoplastic cells. The present invention is useful, inter alia, in the therapeutic and/or prophylactic treatment of cancers such as, but not limited to, solid cancers such as cancers of the colon, stomach, lung, brain, bone, oesophagus, pancreas, breast, ovary or uterus.
USRE42645 Nutritional or therapeutic compositions and methods to increase bodily glutathione levels Nutritional or therapeutic compositions containing glutamic acid, cystine, glycine and a selenium precursor and methods for their utilization to increase glutathione synthesis and thereby enhance the immune system are described.
US20120100120 Performance enhancing composition and method of delivering nutrients An aqueous composition specifically adapted for supporting physical performance. The liquid composition comprises ribose, a saccharide such as glucose or dextrose, coenzyme Q10, ATP, caffeine, and D-pinitol in conjunction with minerals and electrolytes. The orally-consumed liquid composition may be sold in solid form, such as a powder, granulate, or tablet to be added to water or other fluid, or it may be sold as a shelf-stable ready-to-drink liquid. The liquid composition physiologically enhances essential energy stores and provides a supply of ingredients which support physiological generation and regeneration of ATP.
EP2323672A1 Compositions for the prophylaxis and treatment of dermatological/mucosal diseases, and uses thereof The present invention provides a composition containing a) clay material with a negative surface charge; b) magnesium ions either incorporated within the clay material and/or added separately; c) water; d) substantially non-cationic carrier; where the total molar amount of magnesium ions compared to calcium ions is higher than 40% of the total molar amount of calcium ions. The present invention further relates to the use of said composition for the preparation of a medicament for the treatment of skin diseases or skin conditions, where the formation and/ or recovery of epidermal barrier function has beneficial effects.
WO2014071149A1 Heparanase and its uses related to exostoses Methods of treating or preventing exostosis in a subject comprising administering to a subject with exostosis or at risk of developing exostosis an effective amount of an agent that that cleaves heparan sulfate or an agent that increases expression of an enzyme that cleaves heparan sulfate are provided herein.
CN101919862A Application of benzamide derivative to preparing antitumor drug The invention belongs to the gene engineering and chemical field and relates to application of FD4: N-(3-(benzamide)-5-(4-oxo-4H-3,1-benzoxazine-2-yl) phenyl) benzamide to preparing an antitumor drug. The FD4 can obviously inhibit proliferation of tumor cells, is a drug designed aiming to a cell target CYPJ (Cyclophilin J), is not easy to cause the drug resistance and also has special and obvious effect to the tumor cells of a high expression CYPJ protein. Therefore, a small molecular compound is developed as a novel antitumor drug and has obvious tumor killing effect and good specificity, and the FD4 can be developed as the novel antitumor drug and provides a new way and means to treat and cure the tumor.
CN101548996B Compound poplar flower oral liquor and preparation method The present invention provides a compound poplar flower oral liquor. Each 100 ml solution contains medicinal ingredient as follows: ofloxacin 4.0-7.0 g, atropine sulfate 0.03-0.05 g, poplar flower extract liquid 93-96 ml, each 1 ml poplar flowers extract liquid equals to 1.10-1.15 g of poplar flowers raw ingredient. The compound poplar flower oral liquid can prevent and treat diarrhea or intestinal inflammation of the animal efficiently, optimize treating effect. The compound poplar flower oral liquid is added into drinking water for animal in general, each 100 oral liquid is added with 200 jin water, and the patient animal can be cured after taking the oral liquid 2-3 days. The compound poplar flower oral liquid has obvious treating effect and does not relapse after taking.
US8580316 Immune stimulatory infant nutrition A nutritional or pharmaceutical composition comprising fat, protein, carbohydrate, whey and casein is provided. The composition has a weight ratio of casein to whey between 1:1 to 1:2.4 and comprises: a) at least 3 grams arginine per 100 grams protein; b) at least 10 wt. % linoleic acid based on total fatty acids; c) at least 1 wt. % alpha linolenic acid based on total fatty acids; d) at least one long chain-polyunsaturated fatty acid in an amount exceeding 0.1 wt. % based on total fatty acids selected from docosahexaenoic acid, arachidonic acid and eicosapentaenoic acid; e) 5 to 25 wt. % of at least one polyunsaturated fatty acid based on total fatty acids; and 2 to 12 grams indigestible oligosaccharides having a degree of polymerisation of 2 to 100 per 100 gram dry weight of the composition. Methods of treatment by administering the composition are also provided.
US20080214512 Pharmaceutical preparation containing a gestagen, and kit and method for treating endometriosis using the preparation The pharmaceutical preparation for treating endometriosis contains at least 28, preferably 30, daily dose units, each of which contain dienogest, cyproterone acetate, or chlormadinone acetate at a daily dose that is at most twice that required to inhibit ovulation together with one or more pharmaceutical aids and/or carriers. The daily dose units are administered in a method of prophylaxis and/or therapy of endometriosis continuously during a time interval of at least 169 days or 25 weeks, preferably more than two years. The method effectively reduces endometriosis and associated pain, while undesirable side effects including bone density decrease are reduced or eliminated.
WO2011052888A3 (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or pharmaceutically acceptable salts thereof, method for preparing same, and pharmaceutical composition containing same as active ingredients for the diagnosis or treatment of neurodegenerative brain diseases The present invention relates to (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or to the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a pharmaceutical composition containing same as active ingredients for the diagnosis or treatment of neurodegenerative brain diseases. The aryl derivatives of the present invention are (3-fluoro-2-hydroxy)propyl-functionalized to increase the polarity thereof, and therefore the drugs containing the aryl derivatives can easily permeate into the cerebrovascular membrane, thus increasing the effectiveness of the drugs. As the aryl derivatives of the present invention strongly bind to β-amyloid, the aryl derivatives, when labeled with radioisotope, can be used as a diagnostic agent for non-invasively diagnosing early Alzheimer's disease. Further, the aryl derivatives of the present invention bind to low molecular β-amyloid peptide conjugates to inhibit the generation of malignant high molecular β-amyloid plaque, and thus can be effectively used as a therapeutic agent for neurodegenerative brain diseases such as Alzheimer's disease.
WO2007018273A1 Composition for delivering diagnostic agent containing sugar-modified liposome It is intended to provide a composition for delivering a diagnostic agent containing a sugar-modified liposome useful for delivery to the body such as oral administration and a diagnostic agent. The sugar-modified liposome to be used in the composition for delivering a diagnostic agent of the invention preferably has a sugar chain having at least one specific sequence bonded through a linker such as human serum albumin.
US20090110657 Skin care compositions Provided are compositions which are suitable for topical application to mammalian skin for cleansing and anti-microbial properties. In one embodiment, the compositions include an ester of polyalkylene glycol monoazelate monolaurate. It is postulated that bacteria on or in the skin may cleave the ester linkage of a compound according to the present disclosure that is applied to the skin, which causes liberation of the acid moiety from the ester, which acid moiety then inhibits or kills the bacterium. Compositions according to the present disclosure may comprise skin creams, soaps, shampoos and lotions, and are especially effective in treating acne and acne-like skin ebullitions.
CN103232422A A light-sensitive expansionary polymer and a preparation method and applications thereof The present invention discloses a light-sensitive expansionary polymer and a preparation method and applications thereof, belonging to the field of light-sensitive drug carriers. According to the invention, the light-sensitive expansionary polymer shown in formula I is obtained by finally reacting nitroacetophenone after being subjected to reduction and hydroxyl group activation in turn, and introduction of ethanolamine, with methacryloyl chloride. Through a cross-linking agent and an initiator, by employing a microemulsion polymerization method, the light-sensitive expansionary polymer of the present invention is used to encapsulate drugs to obtain light-sensitive drug nanoparticles. Dynamic light scattering (DLS) and scanning electron microscopy (SEM) observations show that the obtained nanoparticles has a size distribution between 100-200nm, the nanoparticles have good stability, and after optical stimulation, the volume of the nanoparticles expands 100-400 times, which can effectively improve the bioavailability of drugs, and prolong the duration of action of the drugs by controlling release of the encapsulated drugs through light.
EP1931661A1 Isoxazolo derivatives as gaba a alpha5 inverse agonists The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula (I) wherein R1 is hydrogen, halogen, lower alkoxy, phenyloxy or benzyloxy; R2 is lower alkyl, (CH2)n-O-lower alkyl or phenyl; R3 is hydrogen or lower alkyl; R4/R5 are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkynyl or -(CHR)n-aryl, unsubstituted or substituted by halogen, lower alkyl or lower alkoxy, -(CH2)n-non aromatic heterocyclic ring, unsubstituted or substituted by one or two lower alkyl groups, -(CH2)n-aromatic heterocyclic rings -(CR2)n-cycloalkyl, unsubstituted or substituted by one to three substituents, selected from the group consisting of hydroxy or lower alkyl, -(CHR)n-O-lower alkyl, -(CR2)n-OH, -(CHR)n-NR’R', or R4/R5 form together with the N-atom to which they are attached the ring - 8-aza-bicyclo[3.2.1] octane, substituted by hydroxy, or - 3,4-dihydro- lH-isoquinoline, or - a non aromatic heterocyclic ring, unsubstituted or substituted by one or two substituents, selected from the group consisting of C(O)O-lower alkyl, lower alkyl, lower alkyl substituted by halogen, cycloalkyl, hydroxy, halogen, N(R)C(O)-lower alkyl, -(CΗ2)n-O-lower alkyl, or by an aromatic heterocyclic ring; R is hydrogen, hydroxy, or lower alkyl, wherein R may be the same or different in case of R2; R’/R' are independently from each other hydrogen or lower alkyl; n is O, 1, 2, 3 or 4; m is 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA Aα5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
CN1915978A Crystal form of lonidamine, preparation method, and composition of containing the crystal form This invention provides a method for preparing lonidamine crystals with the forms of I, II and III, as well as a composition containing lonidamine crystals. The lonidamine crystals have good release performance.
US20060052396 Arylamines for the treatment of conditions associated with gsk-3 The present invention relates to new compounds of formula (I) wherein Z, Y, X, P, Q, R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A, m and n are defined as in any one of claims 1 to 3, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds for the treatment of conditions associated with glycogens synthase kinase-3 (GSK3).
WO2013032096A1 Capric acid having inhibiting effect on osteoclast formation and pharmaceutical composition containing same The present invention provides an osteoclast formation-inhibiting agent containing capric acid as an active ingredient, and a pharmaceutical composition containing capric acid as an active ingredient for preventing or treating diseases due to bone loss. The capric acid, according to the present invention, inhibits the formation of an osteoclast by inhibiting the expression of MCP-1 and the expression of iNOS by means of STAT3(Ser727) activity in a RAW264.7 cell that is LPS-treated. Also, the capric acid according to the present invention reduces the expression of LPS-derived TRAP, which is an osteoclast differentiation marker. The pharmaceutical composition containing the capric acid, according to the present invention, is useful in treating various diseases that are induced from bone loss, wherein the diseases can be selected from a group consisting of osteoporosis, arthritis, and periodontitis. In addition, the pharmaceutical composition containing the capric acid, according to the present invention, is useful in preventing or treating asthma and renal failure.
WO2010081647A2 Sgc stimulators of sgc activators in combination with pde5 inhbitors for the treatment of erectile dysfunction The present invention relates to soluble guanylate cyclase (sGC) and to phosphodiesterases (PDEs) and the pharmacology of sGC stimulators, sGC activators and PDE inhibitors. More particularly, the invention relates to the use of sGC stimulators and sGC activators in combination with PDE5 inhibitors for preparation of medicaments for the treatment of male erectile dysfunction (MED) in particular for the MED treatment of difficult to treat patients and patients not or not fully responding to PDE5 inhibitors.
US20120329862 Novel compound having inhibitory effect on lipase This invention provides, a novel polyphenol compound having lipase inhibitory activity derived from tealeaves, a process for the preparation of the compound, and foods and/or beverages and pharmaceutical drugs containing the compound. Particularly, this invention provides a novel dimer compound of formula: obtained by oxidative polymerization of epigallocatechin-3-O-gallate, a main catechin component of oolong tea, with a tealeaf enzyme (polyphenol oxidase), as well as foods and/or beverages and pharmaceutical compositions containing said novel compound which suppress absorption of dietary lipids and suppresses increase of blood triglyceride.
CN1633996A Tuberculosis therapeutic injection The invention discloses a medicinal injection for treating various tuberculosis, which comprises 15-20% of analysis alcohol and balancing triiodomethane, the preparing process comprises charging analysis alcohol and triiodomethane into ethyl ether, fully dissolving, forming miscible liquid, volatilizing the ethyl ether at normal temperature and under atmosphere pressure, thus forming the powdery mixture of analysis alcohol and triiodomethane.
US20090171103 Triptolide Derivatives for Modulation of Apoptosis and Immunosuppression Variously substituted carbonate and carbamate derivatives of triptolide compounds have good aqueous solubility and convert to biologically active compounds in vivo, at a rate which can be modulated by varying the substitution on the prodrug. The prodrugs are useful as immunosuppressive, anti-inflammatory and anticancer agents.
CN102695709A Crystalline forms of substituted pyrazolopyrimidines The present invention relates to novel co-crystals of pyrazolopyrimidines and a co-crystal former, wherein the co-crystal former is an organic carboxylic acid, preferably selected from the group of gentisic acid, succinic acid and xinafoic acid. The pyrazolopyrirnidkes, and in particular compound A are potent mGluR5 modulators and are useful for the prevention and treatment of acute and chronic neurological disorders, in particular CNS (central nervous system) disorders, which involve excessive glutamate induced excitation.
CN103553973A o-nitroaroyl beta-chloroethyl nitrosourea compounds, preparation and use thereof The present invention discloses o-nitroaroyl beta-chloroethyl nitrosourea compounds represented by a formula 1, a preparation method and a use thereof, wherein R is -COCH2C6H4NO2-o, or -COCH2CH2C6H4NO2-o, or -COCH2OC6H4NO2-o. According to the preparation method, o-nitro aromatic carboxylic acid is adopted as a synthesis raw material and is subjected to acylation, substitution, chlorination and nitrosation to obtain the target compound. The compounds can be used in preparation of tumor treatment drugs, particularly in preparation of breast cancer treatment drugs or glioblastoma treatment drugs or human cervical carcinoma treatment drugs or erythroleukemia treatment drugs.
US7078063 Water soluble extract from plant of Solanum genus and the preparation process thereof, and pharmaceutical composition containing the water soluble extract A water soluble extract from a plant of Solanum genus consists essentially of at least 60%–90% of solamargine and solasonine. A process for preparing the water soluble extract from the plant of Solanum genus involves the steps of hydrolysis with an acid, precipitation with a base, and separation treatments using chloroform, alcohol and water as extraction solvents. The water soluble extract prepared from the process can be directly dissolved in pure or neutral pH water to form a yellowish clear and transparent aqueous solution having a water solubility ranging from 2˜20 mg/ml or higher. The water soluble extract can be used as an active component in a pharmaceutical composition for inhibiting the growth of tumor/cancer cells, in particular liver cancer cells, lung cancer cells and breast cancer cells.
CN101904833A Salvianic acid A medical composition and preparation method thereof The invention relates to a salvianic acid A medical composition and a preparation method thereof. The salvianic acid A can be dissolved in water, but preparations of the salvianic acid A have poor stability, easy oxidization and sensitivity to light and heat, which causes content reduction and impurity increase, thus the guarantee of the stability is a technical difficult. The composition comprises the components of salvianic acid A, a pharmacologically allowable pH regulating substance, a stabilizing agent and an excipient. In a product of the composition, the concentration of the salvianic acid A is 0.5-2,000mg per product, the weight part of the pH regulating substance is the addition used when the pH is regulated to 2.5-7.5, the concentration of the stabilizing agent is 1-0.5mg per product, and the addition of the excipient is 0.049-0.8g per product. The product is used as an injection which has the effects of protecting the cardiac muscle, promoting blood circulation, removing blood stasis, resisting bacteria, diminishing inflammation, enhancing the immunity of the organism, resisting atherosclerosis, reducing blood fat, resisting platelet aggregation, resisting thrombosis, expanding the coronary artery, treating liver injuries, resisting cerebral ischemia injuries, resisting tumors, and the like and also has the treatment effect on pulmonary heart diseases, psoriasis, altitude sickness, and the like.
WO2006033412A1 Alleviator for radiation disorder An alleviator for radiation disorders which is safe even when administered to the living body; and a composition containing the alleviator for radiation disorders. The alleviator for radiation disorders contains α-D-glucopyranosyl-(1→2)-L-ascorbic acid as an active ingredient.
CN103638345A Medicine used for treating lung Qi deficiency, and preparation method thereof The invention discloses a medicine used for treating lung Qi deficiency, and a preparation method thereof. The medicine is prepared from medical ingredients such as radix pseudostellariae, rhizoma alismatis, human placenta, radix ophiopogonis, thunberg fritillary bulb, gecko, ardisiae japonica, and stalactite according to a certain weight ratio. The medicine is capable of nourishing Yin and clearing away the lung heat, expelling phlegm and arresting coughing, and tonifying lung and benefiting vital energy. Treatment effect on lung Qi deficiency is realized quickly, treatment course is short, and no toxic or side effect is caused.
CN1850062A Fatty acid eye nano preparations for dry eye disease The present invention relates to a nano emulsion for curing xerophthalmia and related diseases. The described emulsion composition includes fatty acid, emulsifier and water. Said invention also provides its preparation method.
CN101152388B Medicine for treating scald and burn, and method for preparing the same A medicine for curing burn includes the ingredients (with weight portion) 12 to 18 portion of dragon bone, 16 to 23 portion of angelica, 20 to 20 portion of rehmmania root, 11 to 17 portion of mastic,11 to 18 portion of myrrh, 12 to 18 portion of dragon blood, 5 to 11 portion of carbonized hair, 5 to 11 portion of borneol, 30 to 48 portion of beeswax and 400 to 750 portion of sesame oil; the medicine is put into weighted sesame oil to dip for 1 to 5 days and then the medicine and the oil are fried on fire together; when the medicine is the sesame oil is burnt, the dregs are sieved and the oilin which the dregs are sieved is added with weighted beeswax and borneol to be mixed evenly; the product is finished after being cooled; the medicine is characterized by simple manufacture method, low price and convenient use; moreover, no scar can no left after the burn is cured.
CN101468023B Exemestane tablet and technique for preparing the same The invention relates to aromasin tablet and preparation method of same. The invention reduces the dosage of carboxyrnethyl starch sodium and hyprolose, and increases the dosage of microcrystalline cellulose. The aromasin is micronized which overcomes the shortage of the current technical process. The invention provides products of better quality and dissolution rate, and capable being used in industrial production.
US20090202540 Substituted oxazaphosphorines The present invention relates to new oxazaphosphorine alkylating agents and/or immuno-suppressive agents, pharmaceutical compositions thereof, and methods of use thereof.
EP2292235A2 Methotrexate solutions Use of methotrexate is claimed for the preparation of parenteral medicament to treat inflammatory autoimmune disease, where the methotrexate is added to a pharmaceutically compatible solvent, in a concentration of more than 25 mg/ml. Independent claims are included for: (1) a ready-made syringe and carpule, comprising a formulation of methotrexate, which is added to a pharmaceutically compatible solvent, in a concentration of more than 25 mg/ml; and (2) a pen-injector comprising the carpule. - ACTIVITY : Antiinflammatory; Immunosuppressive; Antiarthritic; Antirheumatic; Vasotropic; Gastrointestinal-Gen; Antiulcer; Antiasthmatic; Neuroprotective; Nootropic; Antipsoriatic. - MECHANISM OF ACTION : None given.
CN101785776B Application of ergot sterone in preparation of medicaments for treating chronic renal failure The invention relates to application of ergot sterone in the preparation of medicaments for treating chronic renal failure. The ergot sterone has the effects of lowering urea nitrogen and serum creatinine, improving the renal function and reducing the pathological damage of adenine metabolites to the kidney. The invention provides a novel medicament for clinically treating chronic renal failure caused by adenine, aristolochic acid, rhubarb and the like.
CN102977118A Novel antibiotic of Gram-positive bacteria and its preparation method and use The invention provides a novel antibiotic of Gram-positive bacteria and also provides a strain Streptomycesspectabilis zgd-Q for producing the novel antibiotic. The strain Streptomycesspectabilis zgd-Q is preserved in the China center for type culture collection On September 13, 2012 and has a preservation number of CCTCC No. M2012328. The strain Streptomycesspectabilis zgd-Q having the preservation number of CCTCC No. M2012328 is cultured and an extract is separated from a fermentation broth and then is purified to form the novel antibiotic. The novel antibiotic has a molecular formula of C39H49NO14, has molecular weight of 755 and [M+K]<+> of 794, has a chemical name of 17-carbonyl-19-methoxy-streptovaricin F, can act on Gram-positive bacteria, has a phenol coefficient of 2.0 to 12.8, and has strong effects of killing Gram-positive bacteria.
EP1389236B1 Immunoglobulin superfamily variants expressed in mesenchymal cells and therapeutic uses thereof Mesenchymal cells are unexpectedly found to express specific truncated versions of immunoglobulin (Ig) superfamily members, namely T cell receptors and related proteins of the immunoglobulin superfamily, as exemplified by the upsilon heavy chain. Mesenchymal T cell receptor and Ig heavy chain gene products either directly or indirectly control hemopoetic stem cells. Antisense therapy and antibodies can be used to reduce TCR and Ig heavy chain mediated functions. Conversely, overexpression of the TCR and/or Ig heavy chain can be used to induce hemopoesis, for example in stem cell transplantation or following chemotherapy.
US20110098324 Prolyl hydroxylase inhibitors The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
US20110243883 Polymeric biolubricants for medical use The present invention provides branched polymers which can be used as lubricants or shock absorbers in vivo. For example, the inventive polymers can be used as viscosupplements, viscoelastics, tissue space fillers, and/or anti-adhesive agents. Also provided are pharmaceutical compositions comprising the inventive polymers and methods of using them including, for example, in the treatment of arthritic and sport-injured knee joints; in reconstruction or cosmetic procedures, intervertebral disc repair, treatment of vocal cord problems, treatment of urinary incontinence, and prevention of adhesion formation following abdominal or gynecological surgery.
CN101606975A Medicine for external use for treating rhinitis and preparation method thereof The invention discloses a medicine for external use for treating rhinitis and a preparation method thereof. The medicine for external use is dropping liquid prepared from the following raw materials according to volume proportion. The method for preparing the medicine for external use comprises the following steps: putting fruits of magnolia flower and centipeda minima with the same weight in a naphtha extractor, adding water with an amount equal to five times of the gross weight of the fruits of magnolia flower and the centipede minma, soaking for 24 hours in sealing manner, distilling, extracting and collecting 800 ml of naphtha next day, secondly distilling and extracting 400 ml of distillate, sequentially adding 30-35 ml of gentamicin sulfate injection, 30-35 ml of dexamethasone injection, 15 ml of naphazoline; after stirring, dissolving and homogenizing, sterilizing by high pressure steam for 40 min, finally packaging as finished products according to an aseptic operation. The medicine has advantages of wide application range, good treatment effect, short treatment period, and low cost and has no side effect.
CN102038954B Water-soluble matrix suitable for preparing retinoic acid water-soluble preparation The invention discloses a water-soluble matrix suitable for preparing a retinoic acid water-soluble preparation, which is prepared by evenly mixing the following components in parts by weight: 50-60 parts of polyoxyethylene (40) stearate, 30 parts of fatty alcohol-polyoxyethylene ether (peregal O) and 10-20 parts of glycerol. The invention also discloses application of the water-soluble matrix inpreparing the retinoic acid water-soluble preparation, namely that the water-soluble matrix is taken as a solvent, the retinoic acid is added into the solvent to prepare into a water-soluble cream body or a water-soluble cylindrical object, wherein the mass percent of the retinoic acid is 0.025-0.1%. The water-soluble matrix of the invention does not contain water, but can be dissolved in water, thus ensuring that the medicinal preparation prepared from the water-soluble matrix can be conveniently cleaned, realizing the condition that the medicines do not need to be touched by hands when the medicinal preparation is applied, and lowering the waste of the medicines and the stimulation to hands.
EP2391629A1 Dimeric pyrrolopyrimidinedione and its use in therapy of respiratory diseases The compound of formula (I) is an inhibitor of human neutrophil elastase, useful for inhalation treatment of pulmonary inflammation.
CN102451180A External medicine for treating skin diseases and preparation method thereof The invention discloses an external medicine for treating skin diseases, which contains coenzyme Q10 and miconazole nitrate as active components, wherein the coenzyme Q10 accounts for 0.01 to 79 percent of the weight of the external medicine, and the miconazole nitrate accounts for 0.01 to 45 percent of the weight of the external medicine. The invention also discloses a corresponding preparation method for the external medicine for treating skin diseases. The implementation of the invention can greatly increase the rate of curing various skin diseases, particularly, for the ringworm of the foot, the cure rate can reach more than 95 percent, and the recurrence rate is less than 10 percent in a year; and moreover, the external medicine also has an excellent effect in treating skin fester caused by burn, scald, cut and the like and promoting the healing of the skin fester.
CN103720653A Vinorelbine submicron emulsion injection and preparation method thereof The invention discloses a vinorelbine submicron emulsion injection and a preparation method thereof. The vinorelbine submicron emulsion injection comprises ingredients of vinorelbine-phospholipid complex, triglyceride, an emulsifier, water, and the like. Molar ratio of vinorelbine to phospholipid ranges from 1:1 to 1:10; and the vinorelbine-phospholipid complex is capable of increasing lipid solubility of vinorelbine, and improving distribution of vinorelbine in oil phase greatly. The vinorelbine submicron emulsion injection containing the vinorelbine-phospholipid complex is capable of reducing irritation of vinorelbine; and drug compliance of patients is improved.
US7064134 4-piperidinyl-substituted, e.g., 4-(2-methyl-4-piperidin-1-yl-quinolin-7-ylmethoxy)-benzonitrile; treating eating disorders and obesity Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
CN102827050A Methylene-thiosemicarbazone-based substituted phenoxy carboxylic acid derivative, and preparation method and application thereof The invention discloses methylene-thiosemicarbazone-based substituted phenoxy carboxylic acid derivatives, a preparation method thereof and application of using the methylenethiosemicarbazone-based substituted phenoxy carboxylic acid derivatives as tyrosinase inhibitors. The general formula of the methylenethiosemicarbazone-based substituted phenoxy carboxylic acid derivatives is shown as formula I, wherein R <1> is selected from hydrogen, one hydroxyl, multiple hydroxyl or alkoxy with one to six carbon; when n is equal to 1-6, R<2> is selected from hydrogen, or when n is equal to zero or 3-6, the R<2> is selected from linear alkyl with one to six carbon.
EP0996438B1 Use of cis-6-hexadecenoic acid esters for treating psoriasis, allergies, auto-immune disorders and dry, sensitive skin According to the invention, cis-6-hexadecenoic acid or its derivatives can be used for preventing and treating psoriasis, allergies and auto-immune disorders, and dry, sensitive skin.
CN1931162A Prduction process and application of ornidazole The present invention discloses production process of ornidazole capsule, and belongs to the field of medicine technology. The production process has increased step of pressing pellet into rod and step of sucking the rod into capsule with special apparatus; and produces ornidazole capsule with high yield, small weight difference, stable disintegrating time and high leaching rate. The present invention also discloses the application of ornidazole in preparing medicine for treating anerobe caused diseases. The filler of the ornidazole capsule has ornidazole as active component and conventional excipient supplementary material. The production process includes the steps of mixing ornidazole and supplementary material, wet pelletizing, drying, drying, pressing into rod, sucking the rod into capsule, packing and inspection.
CN101941918A Cassaine alkaloid analogue, preparation method thereof, drug combination and application thereof The invention relates to a bicyclo-analogue of a cassaine alkaloid shown in the general formulas (I, II), a preparation method of the compound, a drug combination containing the same and an application of the compound in preparing drugs capable of preventing and/ or curing cancer.
US20110014127 Methods for measuring a patient response upon administration of a drug and compositions thereof Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.
WO2013126088A1 Methods of increasing light responsiveness in a subject with retinal degeneration Disclosed herein are methods of increasing retinal responsiveness to light in a subject, such as a subject with retinal degeneration. The disclosed methods include administering one or more compounds that decrease or inhibit γ-aminobutyric acid (GABA) signaling to a subject with retinal degeneration. In some embodiments, the methods include selecting a subject with retinal degeneration and administering a γ-aminobutyric acid C (GABAC) receptor antagonist to the subject. In one example, the GABAC receptor antagonist is (1,2,5,6-tetrahydropyridin-4yl)methylphosphinic acid (TPMPA). In other embodiments, the methods include selecting a subject with retinal degeneration and administering a metabotropic glutamate receptor (mGluR) antagonist to the subject. In one example, the mGluR antagonist is a mGlu1 receptor antagonist (for example, JNJ16259685).
WO2009137681A1 Therapeutically useful substituted hydropyrido [3,2,1-ij] quinoline compounds Disclosed herein are compounds represented by the structural formula (I): therapeutic methods, compositions, and medicaments related thereto are also disclosed.
US20120208817 Novel Dihydropyrimidin-2(1H)-one Compounds as S-Nitrosoglutathione Reductase Inhibitors The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
WO2013124441A1 Use of dialkyl-thiosulfinate and/or thiosulfonate to improve the resistance of an animal infected by a pathogen This invention concerns the use of a compound dialkyl-thiosulfinate and/or a compound dialkyl-thiosulfonate to improve the disease resistance of an animal infected by a pathogen. The pathogen may be a virus, bacteria or apicomplexa. The compound is used in an amount of 1g to 20 g per ton of feed (or 0,5g to 10 g per ton of drink). Preferably, the compound is used in an amount of 1g to 10 g per ton of feed (or 0,5g to 5 g per ton of drink).
US20110098631 Medical devices for treating urological and uterine conditions The present invention relates to implantable or insertable medical devices that treat uterine and urological conditions that cause chronic pelvic pain and other symptoms. In another aspect, the present invention relates to methods of manufacturing such implantable or insertable medical devices.
WO2013127918A1 New therapeutic approaches for treating parkinson's disease The present invention relates to compositions and methods for the treatment of Parkinson's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Parkinson's disease and related disorders targeting the alpha-synuclein aggregation network. In particular, the invention relates to compounds which, alone or in combination(s), can effectively protect neuronal cells from alpha-synuclein aggregates. The invention also relates to methods of producing a drug or a drug combination for treating Parkinson's disease and to methods of treating Parkinson's disease or a related disorder.
US20090239813 Analogs of Alpha Galactosyceramide and Uses thereof There are disclosed compound of formula I, in which R1 represents a hydrophobic moiety adapted to occupy the C′ channel of human CDId, R2 represents a hydrophobic moiety adapted to occupy the A′ channel of human CDId, such that R1 fills at least at least 30% of the occupied volume of the C′ channel compared to the volume occupied by the terminal nC14H29 of the sphingosine chain of α-galactosylceramide when bound to human CDId and R2 fills at least 30% of the occupied volume of the A′ channel compared to the volume occupied by the terminal nC25H51 of the acyl chain of α-galactosylceramide when bound to human CDId R3 represents hydrogen or OH, Ra and Rb each represent hydrogen and in addition, when R3 represents hydrogen, Ra and Rb together may form a single bond, X represents or —CHA(CHOH)nY or —P(═0)(0−)0CH2(CH0H)mY, in which Y represents CHB1B2, n represents an integer from 1 to 4, m represents 0 or 1, A årepresents hydrogen, one of B1 and B2 represents H, OH or phenyl, and the other represents hydrogen or one of B1 and B2 represents hydroxyl and the other represents phenyl, in addition, when n represents 4, then A together with one of B1 and B2 together forms a single bond and the other of B1 and B2 represents H, OH or OSO3H and pharmaceutically acceptable salts thereof; the compounds of formula I are indicted for use in the treatment of a virus, microbial infection, parasite, an autoimmune disease, cancer, allergy or asthma
CA2279319C Benzofurazan compounds which enhance ampa receptor activity Compounds of general structural formula (I) are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors dependent upon AMPA receptors, and in treating conditions, such as memory impairment, in which AMPA receptors, or synapses utilizing these receptors, are reduced in numbers or efficiency. They may also be used to enhance excitatory synaptic activity in order to restore an imbalance between brain subregions, as in treatment of schizophrenia or schizophreniform behavior.
WO2005084689A1 Radix astragli extract and production method and use thereof The invention discloses a Radix astragli extract and production method and use thereof. Such Radix astragli extract mainly comprises astragalus saponin, organic acid and astragalus flavonoid glycoside. Such production method consists of the following steps: hot reflux exacting the astragalus raw materials in alcohol, concentrating to obtain the extract; diluting the extract with water, then through the macroporous resin column until the effluent showing negative in saponin reaction, then eluting with water until the eluent showing negative in saccharide reaction, finally eluting with alcohol until the eluent showing negative in saccharide reaction; the alcohol eluent through recoverymg the alcohol, drying and bruising to obtain such Radix astragli extract. The invention also provides the use of such Radix astragli extract for the manufacture of varied medicaments.
US20110105549 Branched 3- and 6-substituted quinolines as cgrp receptors antagonists The present invention is directed to novel branched 3- and 6-substituted quinoline derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
US20060135583 e.g. 4-[3'-(3''-aminosulfonylpropyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazolidinyl]-2-trifluoromethylbenzonitrile; anti-androgen agent which has a sufficient antagonistic effect and reduced side effect profile The present invention provides a compound represented by formula (I): wherein n is an integer selected from 1 to 20, and R1 and R2, which may be the same or different, each represent a hydrogen atom, or a linear or branched C1-C6 alkyl group, or a salt, a prodrug or a solvate thereof, as well as a drug, a pharmaceutical composition containing the compound, and the like.
EP1706106B1 Use of highly concentrated compositions of selected n-3 fatty acids for the treatment of central nervous system disturbances The use is described of a composition comprising either a) alpha-linolenic acid (ALA, C18:3 n-3) or b) docosahexaenoic acid (DHA, C22:6 n-3) or c) DHA in admixture with eicosapentaenoic acid (EPA, C20:5 n-3), in a ratio of 1:0.5 to 1:1.7, respectively, and/or the pharmaceutically acceptable derivatives and/or precursors thereof; either a) or b) or c) being in a concentration not lower than 70% by weight of the total fatty acids weight in the composition, for the preparation of a drug for the prevention and/or treatment of the disturbances of the central nervous system (CNS) such as epilepsy, schizophrenia, bipolar (manic- depressive illness) and unipolar (major depression) psychiatric disorders, and by degenerative Alzheimer's disease and related forms of dementia.
WO2014118133A1 Pyridine derivatives as soft rock inhibitors The present invention relates to new kinase inhibitors of Formula (I) or a stereoisomer, tautomer, racemic, salt, hydrate, or solvate thereof, and more specifically to ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including Respiratory and Gastro-lntestinal diseases.
US20080305187 Use of Parathyroid Hormone for Treating Periodontal Disease and for Other Dental Applications Method for treating or preventing periodontal disease associated with mild to severe alveolar bone loss, and for improving the prognosis of dental implant procedures by administering human parathyroid hormone to a patient in need thereof.
DE102004033405A1 New 7-phenylamino-quinolone or 1,8-naphthyridone derivatives, useful e.g. for treating type II diabetes or arteriosclerosis, are inhibitors of glycogen phosphorylase 7-phenylamino-(aza)-quinolone derivatives (I) and their salts are new. 7-phenylamino-(aza)-quinolone derivatives of formula (I) and their salts are new. R1 : hydroxy or 1-6C alkoxy, optionally substituted by 1-6C alkoxycarbonyl; R2 : hydrogen, 1-6C alkyl or phenyl; R3 : hydrogen, 1-8C alkyl (optionally substituted by R9), 3-7C cycloalkyl, pyridyl or phenyl (both optionally substituted by R10); R9 : amino, (di)1-6C alkylamino, carboxy, 1-6C alkoxycarbonyl, 3-7C cycloalkyl, heteroalkyl, heteroaryl, phenyl or phenoxy, where phenyl and heteroaryl may be substituted by R11; R10 : fluoro, chloro, bromo, 1-6C alkyl or alkoxy, carboxy, 1-6C alkoxycarbonyl, amino or (di)1-6C alkylamino; R11 : fluoro, chloro, 1-6C alkyl or alkoxy, amino, (di)1-6C alkylamino, carboxy or 1-4C alkoxycarbonyl; X : CR4 or N; R4 and R5 : hydrogen, floro, chloro, bromo, hydroxy, nitro, cyano, 1-6C alkyl or alkoxy, where alkyl may be substituted by chloro, fluoro or bromo; R6 : R4 but not hydroxy; R7 : hydrogen or 1-6C alkyl; R8 : phenyl, optionally substituted by up to 5 of fluoro, chloro, bromo, cyano, nitro, 1-8C alkyl, alkoxy or alkylthio, 2-8C alkenyl, 3-7C cycloalkyl, phenyl, benzyl, benzoyl, amino, (di)1-6C alkylamino, -P(O)(1-4C alkoxy)2 or heteroalkyl, where alkyl and alkenyl may be substituted by fluoro, chloro, bromo, carboxy or 1-4C alkoxycarbonyl; heteroalkyl : heterocyclic, (un)saturated 4-7 membered ring with up to 3 heteroatoms (N, O or S) and optionally ring-substituted by fluoro, chloro, bromo, cyano, nitro, 1-4C alkyl, hydroxy, carboxy or 1-4C alkoxycarbonyl; proviso: excluded are compounds where X : N; R1 = hydroxy; R2-R5 and R7 = hydrogen and R8 = unsubstituted phenyl . [Image] - ACTIVITY : Antidiabetic; Antiarteriosclerotic. - MECHANISM OF ACTION : Glycogen Phosphorylase (GP) inhibitor. The compound ethyl 1-ethyl-6-(4-ethylphenylamino)-7-methyl-4-oxo-1,4- dihydro[1,8]naphthyridine-3-carboxylate when tested at 10 mu M in vitro, caused 14% inhibition of GP.
US7595329 4-{[4-({[(3-isopropyl-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)carbonyl]amino}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid; serotonin receptor agonist; gastroesophageal reflux disease, analgesic, cognition activator; less toxicity, good absorption, and metabolic stability This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
EP1397161B1 Compounds comprising an analgesic molecule linked to a vector The invention relates to compounds comprising an analgesic molecule which is selected from morphine and the derivatives and metabolites thereof and which is vectorised by means of its link to a vector such that said analgesic molecule passes through the hematoencephalic barrier. The invention also relates to the use of said compounds for the preparation of medicaments that are used to treat pain.
US20080139635 Inflammation Therapy A method is provided for treating a patient in need of therapy for central nervous system inflammation comprising administering to that patient a therapeutically effective amount of a cannabinoid agonist having efficacy at the CB2 receptor but having substantially no efficacy at the CB1 receptor at that amount.
WO2010021928A1 Organoarsenic compounds and methods for the treatment of cancer A method for treating a lymphoma selected from non-Hodgkin's and Hodgkin's lymphoma comprising administering an organoarsenic compound having a structure of the formula (I) wherein X is S or Se and R1 and R2 are independently C1-30alkyl (R3, R3', R4, R5, W and "n" are as defined in claim 1 ) in particular where the compound is S-dimethylarsinoglutathione, N-(2-S-dimethylarsinothiopropionyl)glycine, 2- amino-3-(dimethylarsino)thio-3-methylbutanoic acid, S-dimethylarsino-thiosuccinic acid or S-dipropylarsino-l - thioglycerol.
US20080096953 N-(2-{2-[(2-Hydroxy-3-isobutyl-3-methyl-4-oxo-cyclobut-1-enyl)-phenyl-methyl]-6-methyl-1H-indol-3-yl}-1,1-dimethyl-ethyl)-acetamide, for example; useful as chymase inhibitors; treatment of allergy, asthma, peripheral arterial occlusive disease, irritable bowel disease The invention is concerned with novel vinylogous acid derivatives of formula I: wherein A and R1 to R5 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are useful as chymase inhibitors.
CN101613378B Acidic oligosaccharide having weight-reducing and lipid-lowering effects and application thereof The invention relates to an acidic oligosaccharide having weight-reducing and lipid-lowering effects and application thereof. The adopted technical scheme is that a preparation method of the acidic oligosaccharide is as follows: taking pectin water solution with the weight percentage concentration of 1 percent to 2 percent, regulating pH to 2 to 4, decomposing and reacting the solution for 15 minutes to 24 hours at 90 to 120 DEG C to obtain pectin decomposer, treating the pectin decomposer by a hollow fiber membrane or a ceramic filter membrane, recovering oligosaccharide mixtures with the molecular weight of lower than 6000 daltons, recovering the oligosaccharide mixtures with the molecular weight of 200 to 6000 daltons through a nano-filter membrane, carrying out chromatographic separation by utilizing Bio-gel P-2 gel column or SephadexG-25 gel column or DEAE-Sephadex A-25 anion exchange resin, and carrying out gradient elution by utilizing inorganic salt water solution to obtain the pectin acidic oligosaccharide with the contact ratio of 2 to 20. The acidic oligosaccharide prepared by the invention can be applied to weight-reducing and lipid-lowering health food.
US20090176754 Crystalline Form of the Compound A-348441 There is provided a hemihydrate of (3β, 5β, 7α, 12α)-7,12-dihydroxy-3-{2-[{4-[17β-hydroxy-3-oxo-17α-prop-1-ynylestra-4,9-dien-11β-yl]phenyl}(methyl)amino]ethoxy}cholan-24-oic acid in a crystalline form which is characterised by an X-ray diffraction pattern having major peaks at 2θ=6.58±0.2, 8.54+0.2, 12.28±0.2, and 19.68±0.2. This crystalline material is useful in the treatment of conditions associated with an excess of hepatic glucocorticoid response.
CN103127083A Application of Aphanamixoid A to insulin secretion stimulating medicine The invention belongs to the field of pharmacy and discloses application of Aphanamixoid A to preparation of insulin secretion stimulating medicine. The application of the Aphanamixoid A to the preparation of the insulin secretion stimulating medicine is made public for the first time. The skeleton type is fully novel, besides, activity of the Aphanamixoid A in stimulating insulin secretion is surprisingly strong, the possibility that inspiration is obtained from other compounds does not exist, and therefore the Aphanamixoid A has prominent substantive features, and meanwhile, significant progress of the application of the Aphanamixoid A to prevention and treatment of type 2 diabetes mellitus is obviously achieved.
CN101012235A Amino butanetriol salt of cephalosporin compounds and preparing method The invention discloses a pehanorm salt or hydrate with chemical formula as picture (1) and drug composition and application to treat bacterial infection, which comprises the following parts: cefuroxime oxtatromethane, cepham qusong tromethane, cepham thiotepa tromethane, cefoperazone tromethane, cephalothin tromethane, cefotaxime tromethane, cefolading tromethane, cefonixin tromethane, cefameizin tromethane, cefadizine tromethane, cefuroxime tromethane, cefazolin tromethane, cefapamine tromethane, cefazoline tromethane, cefaadid tromethane, cefaoxofluoride tromethane, cefaminol tromethane and their hydrate.
WO2008146917A1 Lincomycin derivatives and antibacterial agents containing the same as the active ingredient Compounds represented by the general formula (1) [wherein A is aryl; R1 is N-(optionally substituted C1-6 alkyl)-N-(optionally substituted C1-6 alkyl)amino-C1-6 alkyl; R2 is hydrogen or optionally substituted C1-6 alkyl; R3 is optionally substituted C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2], or pharmacologically acceptable salts or solvates thereof. These compounds are novel lincomycin derivatives having potent activity against drug-resistant pneumococcus which is a recent problem in the treatment of infectious disease. The compounds can be used as antibacterial agent and are useful in the prevention or treatment of bacterial infectious disease.
US7875614 Phthalazinones Compounds of the formula I, in which R, R1, R2, R3, R4, R5, R6, R7, R8, Z1, Z2, Z3 and Y1 have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours
US20120322874 Pharmaceutical Uses The invention provides a method of treating an angiogenesis-mediated ocular disorder, e.g. ocular neovascularisation, retinal neovascularisation, including neovascularisation following injury or infection, retrolental fibroplasias, and neovascular glaucoma, age-related macular degeneration, diabetic retinopathy, pathologic myopia, ocular histoplasmosis, neovascular glaucoma, retinopathy of prematurity, the after effects of corneal transplantation, control of postsurgical ocular inflammation (e.g. after cataract surgery), cystoid macular edema (CME), herpes keratitis, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor of formula I wherein R, R1, R2, R3, R4, and R5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug esters thereof.
WO2011073218A1 Compositons and methods for inhibiting expression of il-18 genes The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a IL-18 gene. The invention also relates to a pharmaceutical composition comprising the dsRNA or nucleic acid molecules or vectors encoding the same together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of a IL-18 gene using said pharmaceutical composition; and methods for inhibiting the expression of IL-18 in a cell.
US20050176941 Nucleoside analogues whose sugar moieties are bound in s-form and oligonucleotide derivatives comprising nucleotide analogues thereof Compounds of the following general formula (1) and salts thereof: where A represents an alkylene group having 1 to 2 carbon atoms, etc.; B represents an aromatic heterocyclic group which may have a substituent, etc.; R1 and R2 each represent a hydrogen atom, a protective group for a hydroxyl group for synthesis of nucleic acid, a phosphate group, or —P(R4)R5 [where R4 and R5 are the same or different, and each represent a hydroxyl group, a hydroxyl group protected with a protective group for synthesis of nucleic acid, a mercapto group, a mercapto group protected with a protective group for synthesis of nucleic acid, etc.]; and R3 represents a hydrogen atom, a halogen atom, a hydroxyl group, a hydroxyl group protected with a protective group for synthesis of nucleic acid, etc. These compounds are useful for producing oligonucleotide analogues useful for the antisense method, antigene method, etc., and for producing their intermediates.
EP1228202B1 Antisense compositions and cancer-treatment methods A composition comprising an antisense oligomer directed to an mRNA preferentially expressed in stem cells is described together with methods for treating stem cells with such a composition to increase the number of lineage committed progenitor cells and their progeny, and/or slow the growth of cancer cells. Also described is the use of such compositions and antisense oligonucleotide-treated stem cells as a medicament.
US20130059808 Aminoglycoside derivatives The present invention relates to antimicrobial agents. Some embodiments include compounds, compositions, methods of preparation, and methods of treatment using new aminoglycosides and aminoglycoside derivatives.
WO2014093726A1 Methods of treating portal hypertension The present invention provides methods for treating or preventing portal hypertension comprising administering to a patient in need of such treatment or prevention at least one Rev-erb modulating agent (REMA) in an amount effective to treat or prevent said portal hypertension. The REMA can be SR6452 or a related compound, such as SR9009 or SR9011. The amount of the REMA administered can comprises a quantity sufficient to modulate Rev-erbα expression, activity, and/or subcellular location and/or to inhibit or reverse hepatic stellate cell (HSC) activation and contractility.
US20050269722 Process for the preparation of pharmaceutical microcapsules with enhanced taste-masking and high dissolution rate Process for the production of microcapsules containing a drug and comprising a layer of ethylcellulose and a layer of an acrylic polymer and microcapsules produced thereby.
CN101265199A Method for the preparation of escitalopram A novel method is provided for the manufacture of escitalopram. The method comprises chromatographic separation of the enantiomers of citalopram or an intermediate in the production of citalopram using a chiral stationary phase such as Chiralpak AD or Chiralcel OD. Novel chiral intermediates for the synthesis of Escitalopram made by said method are also provided.
CN101209254A New use of polyhydroxy galloyl-beta-D-glucose derivatives The invention relates to a usage of polyhydroxy galloyl-Beta-D-glucose derivatives or the medicinal salts in anti-helicobacter pylori, and the invention also relates to a usage of drugs which contain at least one extract of polyhydroxy galloyl-Beta-D-glucose derivative used for the prevention and/or treatment of diseases which are caused by helicobacter pylori.
EP1915375A1 Derivatives of 5-pyridinyl-1-azabicyclo[3.2.1]octane, preparation method thereof and use of same in therapeutics The invention relates to compounds having general formula (I), wherein R represents a group that is selected from pyrazolyl, imidazolyl, triazolyl, oxazolyl, oxadiazolyl, thiazolyl, isothiazolyl, thiadiazolyl, tetrazolyl, said group being optionally substituted by one or more groups selected from among halogen atoms, groups (C1-C6)alkyl, (C1-C6)alkoxy, trifluoromethoxy, trifluoromethyl, nitro, cyano, hydroxy, amino, (C1-C6)alkylamino or di(C1-C6)alkylamino, with a single or double carbon-carbon bond between positions 3 and 4 of the azabicyclooctane ring; in the form of a base, an acid addition salt, a hydrate or a solvate. The invention also relates to the method of preparing said compounds and to the use of same in therapeutics.
CA2541852A1 Bone morphogenetic protein (bmp) 2a and uses thereof The present invention provides compositions and methods for alleviation or reduction of the symptoms and signs associated with damaged neuronal tissues whether resulting from tissue trauma, or from chronic or acute degenerative changes. In particular, some embodiments of the present invention provide one or more pharmaceutical compositions comprising as an active ingredient a BMP2A inhibitor further comprising a pharmaceutically acceptable diluent or carrier. An additional embodiment provides a method for reducing damage to the central nervous system in a patient who has suffered an injury to the central nervous system, comprising administering to the patient a pharmaceutical composition in a dosage sufficient to reduce the damage. Yet another embodiment provides of the use of a BMP2A inhibitor for the preparation of a medicament for promoting or enhancing recovery in a patient who has suffered an injury to the central nervous system. Preferable inhibitors according to some embodiments of the invention are siRNA molecules and neutralizing antibodies. An additional embodiment provides a method for identifying a chemical compound that modulates apoptosis. Further, a process for diagnosing a neurodegenrative disease or an ischemic event in a subject is provided. The preferred methods, materials, and examples that will now be described are illustrative only and are not intended to be limiting; materials and methods similar or equivalent to those described herein can be used in practice or testing of the invention. Other features and advantages of the invention will be apparent from the following detailed description, and from the claims.
US20080214606 Methods for the Identification and Use of Compounds Suitable for the Treatment of Drug Resistant Cancer Cells The present invention relates to novel methods for the identification of compounds useful for the treatment of drug resistance, and to novel treatment methods using the identified compounds.
WO2009153500A3 Plant-based compositions and uses The present invention relates to novel plant-based compositions and to uses thereof, in particular as a food supplement or additive or as an allopathic or homeopathic medicament. The invention relates more particularly to compositions comprising at least one extract of cinnamon and one extract of basil, and to uses thereof in the dietary, nutraceutical or pharmaceutical field. The compositions of the invention can be used in particular for treating or preventing urinary infections, or for improving the condition of patients suffering from a urinary infection. The present invention also relates to the use of an extract of cinnamon in the form of an essential oil, alone or in combination with at least one other plant extract, for the manufacture of a composition for use in treating a urinary infection.
EP2301567A1 Selective immune down regulation (SIDR) for transplantation Novel immune modulating processes are provided in which the immunological state of a subject including mature subjects, mammals and humans, are down regulated in a selective manner, and as a subset in a dominant manner. The novel immunological state termed SIDR for selective immune down regulation is usefully applied to the immunological modulation or regulation of gene delivery components, artificially expressed genes, gene delivery systems and expression products of artificially introduced genes by such delivery systems, and infectious agents. SIDR is also useful when combined with other immune modulating treatments such as general immune suppression and anti-apoptosis. SIDR may also be used to selectively down regulate the immune response system of a subject to a wide variety of noncellular immunogenic components and to native antigens. Other processes for producing immune suppression by administering macromolecules or compounds to a subject so as to obtain or effect SIDR are also provided. Kits for carrying out the novel processes are also provided.
WO2007135703A3 Patch for the treatment of the cellulite and localized adiposity Described herein is a patch containing phosphatidylcholine in an appropriate amount for the treatment of cellulite and localized adiposity.
US20080221107 6-(4-chlorophenyl)-3-{4-[(3R)-3-hydroxypyrrolidin-1-yl]-3-methoxyphenyl}thieno[3,2-d][1,2,3]triazin-4(3H)-one; Melanin concentrating hormone receptor antagonist; obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and neurological disorders Compounds of formula (I), processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders and to pharmaceutical compositions containing them.
US7259163 Viricides against herpes virus Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.
CN101297867B Cigarette for quitting drug and preparation thereof The invention discloses a cigarette for detoxification, wherein, tobacco shreds are composed of tobacco and lotus leaves absorbing ingredients of a detoxification drug, and the tobacco accounts for 10 to 50 percent of the total mass of the tobacco shreds. The invention further discloses a preparation method of the cigarette for detoxification. The cigarette for detoxification of the invention canallow drug aerosol to be absorbed by the human inner mucosa in the ionic state with the help of a smoking mode of the cigarette by the people, thus having significant efficacy, rapid effectiveness and facilitating the fine adjustment and control of the dose of the psychotropic drug; furthermore, the preparation method is simple and easy to realize, thus having broad market prospect.
WO2008029871A1 Nerve fiber degeneration inhibitor It was verified that by an experiment using a gene-silencing nucleic acid (GalNAcST siRNA), which is a substance having an “action of inhibiting the synthesis” of chondroitin sulfate proteoglycan (CSPG), chondroitinase ABC, which is a substance having an “action of promoting the degradation” of CSPG and C4-sulfatase, which is a substance having an “action of desulfating” CSPG, a substance that “inhibits the production or accumulation of CSPG” in a totally different route of a totally different property has an effect of inhibiting nerve fiber degeneration. It was revealed that the substance that “inhibits the production or accumulation of CSPG” which is a feature common to these is useful for inhibiting nerve fiber degeneration. The invention relates to a nerve fiber degeneration inhibitor containing a substance that inhibits the production or accumulation of CSPG as an active ingredient and a screening method for the nerve fiber degeneration inhibitor.
US20090176816 Drug composition for treating 2 type diabetes and diabetic chronicity complications A drug composition for treating type 2 diabetes and diabetic chronicity complications is disclosed. The composition is composed of mangiferin and berberine in a certain ratio. The composition has a preferable hypoglycemic and hypolipidemic effect compared with mangiferin and berberine which is used alone
WO2012116247A1 Hsp90 inhibitory compounds in treating jak/stat signaling-mediated cancers Methods for treating a subject with cancer mediated through dysregulated, aberrant, or defective JAK/STAT signaling, are provided, comprising determining the level of the JAK/STAT signaling in a sample derived from a subject in need of treatment, wherein the presence of dysregulated, aberrant, or defective JAK/STAT signaling is indicated, administering to the subject an effective amount of a triazolone compound as described herein.
CN101653498B Nano-herb micro-pills for removing eel poisoning and preparation method thereof The invention relates to nano-herb micro-pills for removing poisoning and a preparation method thereof. The micro-pills comprises the following active components in percentage by weight: 2.8 to 3.2 percent of terminalia leaf, 5.8 to 6.2 percent of serissa serissoides leaf, 7.0 to 7.4 percent of olive leaf, 3.4 to 3.8 percent of mono maple leaf, 10.0 to 10.4 percent of wild chrysanthemum leaf, 39.8 to 40.2 percent of nano-silicon dioxide modified by organic ligand, 23.8 to 24.2 percent of microcrystalline cellulose and 5.8 to 6.2 percent of chitosan. The nano-herb micro-pills can effectively reduce contents of heavy metal elements and toxic substances, such as malachite green, nitrofurans, carbostyril and the like in eel bodies, contributes to the repair of eel livers, adopts pure plant components as raw materials without new residues in the eel organism, has high safety, and simultaneously meets the national requirement of environmental protection.
EP1692143B1 Tricyclic indole hydroxyethylamine derivatives and their use in the treatment of alzheimer's disease The present invention relates to novel hydroxyethylamine compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity of formula (I), processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease. Formula (I) wherein, inter alia, A-B represents -NR5-SO2- or -NR5-CO-; R5 represents hydrogen, C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl, C3-10 cycloalkyl, -C0-6 alkylaryl, -C0-6 alkyl-heteroaryl, -C0-6 alkyl-heterocyclyl, -C3-10 cycloalkyl-aryl or -C3-10 cycloalkyl-heteroaryl; -W- represents -CH2-, -(CH2)2-, -(CH2)3-, -C(H)=C(H)- or -CH2-C(H)=C(H)-; X-Y-Z represents -C=CR8-NR9-;
CN103570634A Erlotinib hydrochloride polymorphic substance and preparation method thereof The invention discloses an erlotinib hydrochloride polymorphic substance and preparation method thereof. Specifically, the invention discloses a polymorphic substance of erlotinib hydrochloride semihydrate compound with purity of 95% and more and a preparation method of the polymorphic substance. The preparation method provided by the invention is simple to operate and suitable for industrial production. The polymorphic substance prepared through the preparation method is good in stability and high in water solubility.
EP1115416B1 Use of substances with oxytocin activity in order to create cell regeneration The present invention relates to the use of substances with oxytocin activity in order to improve cell regeneration. It also relates to a pharmaceutical composition comprising at least one substance with oxytocin activity in order to improve cell regeneration.
US20090082364 Deuterium-enriched levocedtirizine The present application describes deuterium-enriched levocetirizine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN101284006A Medicine composition for treating eye disease The invention discloses a pharmaceutical composition for treating eye diseases, which comprises a macrolides compound and surfactant. The surfactant is hydrophilic surfactant with HLB more than or equal to 10, and is selected from polyoxyethylene fatty acid ester, polyoxyethylene fatty alcohol ether, polyoxyethylene alkyl phenyl ether, polyoxyethylene-polyoxypropylene copolymer/block copolymer and the mixture thereof. The composition can be used for treating immune-related eye diseases and xerophthalmia.
WO2009065395A2 Novel use of omega-3-fatty acid(s) The invention relates to the use of omega-3-fatty acid(s) in means for pain relief. Said means preferably comprise highly unsaturated omega-3-fatty acid(s) that contain, above all, EPA and/or DHA. Preferably, the omega-3-fatty acid is administered in a high dose of more than 2g, in particular more than 3 to 4g, for pain relief.
US20130071491 Extruded Legume Food Products Containing Yeast Autolysate An extrusion process for producing a uniform and highly expanded food product is disclosed with nutritional yeast and chromium. The uniform expansion ratio possessed by the extruded product provides a consistent texture and has application in a wide variety of food consumables, ranging from snacks to breakfast cereals.
US20110104121 Female Reproductive Tract and Anal Prophylaxes The present invention provides methods for boosting mucosal immunity in the female reproductive tract of pre- and post-menopausal women using a TGF-beta inhibitor, a Selective Estrogen Receptor Modulator, and/or a recombinant commensal bacterium that expresses endogenous microbicides into the intestinal tract or reproductive tract of a subject. It also provides methods for boosting innate and adaptive immunity by providing a glucocorticoid. Methods for preventing sexually transmitted infections including HIV infection are also provided.
EP2348021A1 Rotaxane compound and antitumor agent An antitumor agent which is not easily excreted from tumor cells and is suitable for a topical treatment. Specifically disclosed is a rotaxane compound with contains a compound represented by chemical formula 1 as the base structure. (In chemical formula 1, m ≥ 2, n ≥ 3, and X represents an anionic molecule or an anionic atom
WO2013023104A1 Chlorobis copper (i) complex compositions and methods of manufacture and use A method of manufacturing an anhydrous copper complex of formula C12H10CICuN2O4 and methods of treating neuromuscular and other diseases, including but not limited to fibromyalgia, multiple sclerosis, muscular dystrophy, rheumatoid arthritis, pain, fatigue, sleeplessness, loss of fine motor control, speech loss, inflexibility, Alzheimer's, dementia, amyotrophic lateral sclerosis, depression, lyme disease, lyme disease co-infection, gastroparesis (GP), myopathy, chronic inflammation and/or incontinence. The anhydrous copper complex preferably is administered in a pharmaceutical and/or dietary supplement composition of the invention.
US20120264761 Aminobenzoquinazolinone M1 Receptor Positive Allosteric Modulators The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
US20050245575 1-((5-aryl-1,2,4-oxadiazol-3-yl) benzyl)azetidine-3-carboxylates and 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl) pyrrolidine-3-carboxylates as edg receptor agonists The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
US20070185095 Fused heterocyclic compounds and their use as metabotropic glutamate receptor antagonists The present invention is directed to compounds of formula: (I); wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, R1, R2, R3, R4, and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds for treating gastrointestinal disorders.
WO2014082724A1 Aqueous oral solutions of steroid hormones and hydroxypropyl-beta-cyclodextrin with optimised bioavailability The present invention concerns the preparation and the therapeutic use of aqueous solutions of Progesterone or Testosterone, complexed with hydroxypropyl-3-cyclodextrin (HPβCD) that are suitable for oral administration. The solutions are characterised by a specific molar ratio between HPβCD and the hormones such as to ensure high hormone plasma levels, following oral administration, thanks to the optimisation of their solubility, permeability, metabolic stability and ultimately, bio availability. The formulation object of the present patent makes it possible to achieve effective plasma concentrations following oral administration of lower doses of hormone with respect to oral formulations currently on the market (e.g. Prometrium, Andriol) to the advantage of greater safety and compliance of the patients.
US20090197821 Compositions and methods for the delivery of poorly water soluble drugs and methods of treatment The present embodiment of the invention is generally directed to compositions comprising suspensions of poorly water-soluble compounds recrystallized in nanoparticulate sizes ranging from 0.1 to 5 μm. In addition, the embodiment of the invention is directed to methods for preparation and administration of these compositions to a patient for prevention and treatment of disease states. In particular, the embodiment of the invention is directed to compositions comprising suspensions of poorly water-soluble compounds, such as antimitotics and antibiotics, in nanoparticulates and methods of prevention and treatment of chronic disease states, such as cancer, by intraperitoneal and intravenous administration of such compositions
CN102665715A Compositions for treatment of cystic fibrosis and other chronic diseases The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one compound of Formula I, Formula II, or Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
WO2006092032B1 PHARMACEUTICAL COMPOSITIONS CONTAINING 1-METHYL-3,6,7,8-TETRAHYDROPIRAZOLO[3,4-b]PIRROLO[4,3-d]PYRIDINE-6,8-DIONE DERIVATIVES, USE, AND PROCESS FOR PREPARING THEM The present invention is related to new derivatives of 1-methyl-3,6,7,8- tetrahydropirazolo[3,4-b]pirrolo[4,3-d]piridin-6,8-dione nucleus, preferably heterocyclic derivatives, acting as hypnotics and analgesic in the central nervous system, being useful in the treatment of anxiety and central hyperalgesia, including: anxiety relief, central hyperalgesia relief in mammals, preferably humans. It is also described pharmaceutical compositions containing said compounds and preparation processes.
WO2012099375A2 P47phox or p67phox-targeting therapeutic agent for stress disorders, and method for screening for same The present invention relates to a method for preparing a stress sensitivity relieving agent, to a stress-reducing food or feed containing the stress sensitivity relieving agent, to a pharmaceutical composition for preventing or treating stress disorders, to a method for preventing or treating stress disorders, to a method for screening for the stress sensitivity relieving agent, to a method for providing information for diagnosing stress disorders caused by sensitivity to stress or chronic stress, and to a kit for diagnosing a stress level. According to the present invention, drugs using a mechanism of inhibiting the expression of p47phox or p67phox may be developed, and drugs screened for by the method of the present invention may particularly prevent or treat depression, neurodegenerative brain diseases, etc., the symptoms of which may be caused or exacerbated by chronic stress.
US20100048543 Pyrimidine compounds having ties (tek) inhibitory activity The invention relates to a compound of the Formula I or salt thereof wherein Rx, Ry, Rz, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.
CN103110592A Freeze-drying composition for injection and preparation method thereof The invention discloses a freeze-drying composition for injection and a preparation method thereof. The composition comprises pantoprazole or salt or a single optical isomer and sodium D-glucuronate thereof. The weight ratio of pantoprazole or salt or the single optical isomer and sodium D-glucuronatet thereof is 1:0.05-1.5.
US20090124632 Methods and kits related to the topical administration of quinolone antibiotics° The present invention is generally directed to the treatment of dermatological bacterial infections, burns and wounds. It is more specifically directed to the treatment of such infections, burns and wounds using one or more quinolone antibiotics. In one method of treatment aspect, an aqueous solution containing Ciprofloxacin-HCl is topically applied to the skin of a patient exhibiting a dermatological disorder. In another method of treatment aspect, an ointment containing Ciprofloxacin-HCl is topically applied to the skin of a patient exhibiting a dermatological disorder.
US20120015899 Modified plant virus particles and uses therefor Aspects of the invention provide modified virus-like particles that are designed for therapeutic applications. In particular, aspects of the invention provide CCMV coat proteins that are modified to generate virus-like particles, including mosaic virus-like particles, that can package and/or deliver one or more diagnostic and/or therapeutic agents. The invention also provides methods for treating subjects with one or more modified virus-like particles.
CN103539801A Podophyllotoxin derivative as well as salt, preparation method and application thereof The invention discloses a podophyllotoxin derivative I or pharmaceutically acceptable salt thereof. In the derivative, R1, R2 and R3 are independently selected from hydrogen, nitryl, halogen, trifluoromethyl and C1-C6 alkoxy. The invention also discloses a method for preparing the podophyllotoxin derivative I, which comprises the step of performing a condensation reaction between a compound II and a compound III in a solvent under the action of a condensing agent and alkali. The invention also discloses application of the podophyllotoxin derivative I or pharmaceutically acceptable salt thereof in the aspect of preparation of anti-tumor medicaments. The podophyllotoxin derivative I is a novel compound with anti-tumor activity, provides a new research direction for research and development of anti-cancer medicaments, and expands the research range of podophyllotoxin derivative anti-cancer medicaments.
WO2013024282A3 Inhibitor or down- regulator of the expression of one or both of tbk1 ikk-epsilon for use in the treatment of pi3kinase dependent cancer The invention provides a compound that is an inhibitor of one or both of TBK1 and IKKε, or a down-regulator of the expression of one or both of TBK1 and IKKε, for use in a method of treating a cancer that is dependent on the PI3kinase pathway. The invention further provides a method of treating cancer in an individual in whom the cancer is dependent on the PI3kinase pathway, comprising administering to the individual a compound that is an inhibitor of one or both of TBK1 and IKKε, or a down-regulator of the expression of one or both of TBK1 and IKKε.
US20120172339 Angiogenic resorcinol derivatives Novel resorcinol derivatives and methods of preparation and use are presented. These compounds can stimulate angiogenesis as a biological function triggered by the activation of one cannabinoid receptor distinct from CB1 and CB2. Thus, these compounds are specific ligands for one cannabinoid receptor distinct from CB1 and CB2. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.
US20100098688 Method for diagnosis of a disease involving an anti-at1-receptor antibody The present invention relates to a method for diagnosis of a disease selected from the group of diabetes, vasculitis, collagenosis, an inflammatory rheumatic disease and arteriosclerosis wherein, presence or absence of an anti-AT1-receptor antibody is determined in a sample from a patient to be diagnosed and wherein, the presence of an anti-AT1-receptor antibody is indicative of the disease. The invention further relates to the use of an inhibitor of an anti-AT1-receptor antibody or an inhibitor of an AT1-receptor for the production of a medicament as well as plasmapheresis of blood for the removal of anti-AT1-receptor antibodies.
US8410110 9-(piperazinylalkyl) carbazoles as Bax-modulators Piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders, renal hypoxia, hepatitis and AIDS, where the piperazine compounds are represented by formula (I) and the terms R0, R1, R2, R3, k, l, m, n, and X are defined herein:
CA2329005C Folic acid-containing pharmaceutical compositions, and related methods and delivery systems This invention provides folic acid-containing pharmaceutical compositions comprising either an oral contraceptive or a hormone replacement composition. This invention also provides methods of administering folic acid to a subject using the instant pharmaceutical compositions. Finally, this invention provides a drug delivery system useful for administering the instant pharmaceutical compositions.
US6855719 Nitrogen compounds such as 2-(3-Chloroanilino)-4-(2-methyl-imidazo(1,2a)pyrid-3-yl)pyrimidine, used as cyclin dependent kinase inhibitors or as anticarcinogenic agents A compound of formula (I) wherein Ring A is imidazol[1,2a]pyrid-3-yl or pyrazolo[2,3a]pyrid-3-yl; R2 is as defined within; m is 0-5; wherein the values of R2 may be the same or different; R1 is as defined within; n is 0 to 2, wherein the values of R1 may be the same or different; Ring B is phenyl or phenyl fused to a C5-7cycloalkyl ring; R3 is as defined within; p is 0-4; wherein the values of R3 may be the same or different; R4 is as defined within; q is 0-2; wherein the values of R4 may be the same or different; and wherein p+q≦5; or a pharmaceutically acceptable salt or an in vivo hydrolyzable ester thereof is described. The use of compounds of formula (I) in the inhibition of cell cycle kinases CDK2, CDK4, and CDK6 are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
US8226972 Vaginal delivery of drugs Drug delivery compositions which are suitable for vaginal administration for the treatment of diseases and disorders in the urogenital tract are described. The compositions may be in the form of a tablet, liquid suspension or dispersion, dried powder, topical ointment, cream, foam, suppository, or aerosol. The drug delivery compositions are administered directly to the vagina and do not require the use of a solid device. This method of administration reduces the systematic levels of the drugs.
CN1810252A New pharmaceutical use of echinacoside The present invention discloses one new pharmaceutical use of compound, and is especially the new pharmaceutical use of echinacoside in preparing medicine for treating dementia and medicine for treating Parkinson disease. The present invention discloses the functions of echinacoside in improving learning memory disorder, improving the compatibility of autonomous movement, protecting neure against damage, etc.
CN102697706A Sodium dimereaptopropane sulfonate injection and capsule and preparation method thereof The invention provides a sodium dimereaptopropane sulfonate injection and a capsule and a preparation method thereof. The preparation of the sodium dimereaptopropane sulfonate injection is peformed under the condition that sterilization is conducted for 10-20 minutes at the temperature of 121 DEG C or under the aseptic condition. The sodium dimereaptopropane sulfonate capsule comprises 0.09-0.11g/grain of sodium dimereaptopropane sulfonate. The preparation method comprises the steps of (1) weighing sodium dimereaptopropane sulfonate and using a 100-mesh sieve to sieve the sodium dimereaptopropane sulfonate, (2) weighing an auxiliary material and using the 100-mesh sieve to sieve the auxiliary material, (3) mixing the sodium dimereaptopropane sulfonate and the auxiliary material and using the 100-mesh sieve to sieve a mixture, and (4) calculating packable grain weight and filling the mixture into the capsule. The sterility assurance level in the preparation process of the sodium dimereaptopropane sulfonate injection is ensured to meet provisions of letters No. 7 (2008) of the registration department of the state supervision and administration bureau of food and drug--on Notice of Issuance of Basic Technical Requirements for Chemical Medicine Injection and Multi-component Biochemical Injection, and new application of the sodium dimereaptopropane sulfonate injection for treating hepatolenticular degeneration is provided. By means of the sodium dimereaptopropane sulfonate capsule and the preparation method, the problem that heavy metal poisoning sufferers are not suitable for injection dosing or long-term injection dosing is solved.
CN103263415A Levo pantoprazole sodium composition for injection and preparation method thereof The invention relates to the field of medicines for treating gastric ulcer, and in particular relates to levo pantoprazole sodium composition for injection and a preparation method of the levo pantoprazole sodium composition. The levo pantoprazole sodium composition comprises the effective components of medicines in parts by weight: 20-23 parts of levo pantoprazole sodium, 48-52 parts of mannitol, 0.5-1 part of ethylene diamine tetraacetic acid (EDTA)-CaNa and 1,400-1,600 parts of injection water. The method for preparing the levo pantoprazole sodium composition for injection comprises the following steps of: dissolving mannitol and EDTA-CaNa; regulating a pH value to be between 10.5 and 11.5; reducing the temperature and dissolving levo pantoprazole sodium; circularly filtering and decarburizing; degerming; and freeze-drying to obtain a finished product. The levo pantoprazole sodium composition for injection is low in cost and simple in process, and has a good curing effect; and moreover, the side effect is basically avoided and the using amount is reduced.
USRE39585 Administering streptococcus thermophilus in admixture withLactobacillus brevis, Lactobacillus acidophilus, Lactobacillus plantarum, Bifidobacterium infantis, Bifidobacterium longum or Bifidobacterium breve This invention provides materials and procedures for the delivery of selected strains of bacteria and/or oxalate-degrading enzymes to the intestinal tracts of persons who are at increased risk for oxalate related disease because they have lost, or have inadequate concentrations of these bacteria. The administration of these bacteria and/or the relevant enzyme removes oxalate from the intestinal tract and thus reduces the amount of oxalate available for absorption and reduces the risk for oxalate related disease.
US7776850 respiratory tract mucositis; administering an antifungal agent and an antibacterial agent, wherein the treatment does not involve the cessation of use of emollients The present invention provides methods for the treatment of respiratory tract mucositis in individuals in need of such treatment, the method comprising the systemic administration to the individual of therapeutically effective amounts of at least one anti-fungal agent and at least one anti-bacterial agent, wherein the treatment does not involve the cessation of use of emollients by the individual. The present invention also provides compositions suitable for use in the treatment of respiratory tract mucositis.
US20080045483 such as 4-{2-[2-(4-chlorobenzenesulfonylamino)phenyl]ethyl}benzoic acid; hyperglycemic agents The invention relates to compounds of general formula (1): in which R1, R2, R3, R4, R5, A, B, D and E are as defined in Claim 1, and also to the preparation process therefor and the therapeutic use thereof. These compounds can be used in the treatment of pathologies associated with hyperglycaemia.
US20100215707 Activated creatinine and precursors thereof as antibacterial agents, compositions and products containing such agents and uses thereof Creatinine, creatinine precursors or the pharmaceutically acceptable salts thereof are activated to function as an antibacterial agent which has broad spectrum activity and is beneficially used in a variety of applications, such as antimicrobial wound dressings, compositions for topical delivery of the antibacterial agent and for preventing and/or inhibiting the occurrence or spread of bacterial infection, as well as the growth of odor-causing bacteria, to name a few.
US20120294937 New pharmaceutical dosage form for the treatment of gastric acid-related disorders According to the invention there is provided a capsule for peroral administration to the gastrointestinal tract containing (a) a pharmacologically effective amount of a PPI or a pharmaceutically acceptable salt thereof and an enteric substance positioned to protect the PPI or salt thereof from the acidic environment of the stomach, and (b) a plurality of granules comprising a pharmacologically effective amount of a micronised H2RA or a pharmaceutically acceptable salt thereof, a disintegrant and a filler The capsules of the invention are particularly useful in the treatment of gastric acid secretion-related disorders, such as gastro-esophageal reflux disease.
WO2010065443A1 Synthesis and novel salt forms of (r)-5-((e)-2-(pyrrolidin-3-ylvinyl)pyrimidine The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
CN101317993A Externally used plaster medicine for children's urorrhea and frequent micturition The present invention relates to an external use plaster for curing child enuresis and frequent urination. The present invention is characterized by extracting a concentrated solution from corn stigma, flatstem astragalus seed, ihih fruit, gardenia and Chinese dodder; preparing the concentrated solution into an extract and evenly mixing and stirring the extract with borneol and matrigel; forming an ointment and coating the ointment on an adhesive tape to obtain the plaster.
US20120316129 Liquid dressing containing chitosan derivative and preparation method thereof The invention relates to a liquid dressing containing a chitosan derivative, comprising the following components in percentage by weight: 1-5% of CMCS (carboxymethyl chitosan), 0.1-0.5% of collagen albumen powder, 10-15% of humectant, 0.2-2% of antibacterial agent, 2-10% of penetration enhancers and the balance of deionized water. The liquid dressing is obtained by mixing the components in sequence, stirring evenly and bulking. The liquid dressing has the advantage of good biocompatibility, good antimicrobial, antiphlogistic and hemostatic effects and high biological safety, and is convenient to use.
US6864277 Brain diosrders; cardiovascular disorders; central nervous system disorders; psychological disorders The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the Vreceptors or both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to a process for preparing them, to the intermediate compounds of formula (II) which are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.
WO2012136385A8 6,7-dihydro-[1,3,4]thiadiazolo-[3,2-a][1,3]diazepin derivative and pharmaceutical composition containing the same as neuromuscular blocker or skeletal muscle relaxant, and method for the preparation The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as neuromuscular blocker or skeletal muscle relaxant.
CN103271903A Novel medical use of icaritin and cycloicaritin as well as composition thereof The invention discloses novel medical use of icaritin and cycloicaritin as well as composition thereof in preparation of a drug of an alpha-glucosidase inhibitor. The composition can be prepared from herba epimedii crude drugs which are matched according to a certain ratio after being respectively extracted to prepare, and also can be obtained in a chemical synthesis manner. The icaritin and the cycloicaritin can be respectively prepared into a hypoglycemic drug in a monomer form, and can be prepared into the hypoglycemic drug in a manner of the composition according to a certain ratio.
EP1769804A2 Method of increasing bone toughness and stiffness and reducing fractures The invention relates to a method for increasing the toughness and/or stiffness of bone and/or reducing the likelihood and/or severity of bone fracture by administering a parathyroid hormone. The method can be employed to increase toughness or stiffness of bone at a site of a potential or actual trauma, such as the hip or spine of a person at risk of or suffering osteoporosis. The method of the invention can reduce the incidence of vertebral fracture, reduce the incidence of multiple vertebral fractures, reduce the severity of vertebral fracture, and/or reduce the incidence of non-vertebral fracture.
CN102028693A Rectal administration composite containing 5-phosphodiesterase inhibitor The invention discloses a rectal administration composite containing a 5-phosphodiesterase inhibitor (PDE-5i). The rectal administration composite contains an effective quantity of the PDE-5i or pharmaceutically acceptable salts, esters and hydrates thereof or pharmaceutical precursors thereof, active metabolites, and the like and contains the following components by weight ratio: PDE-5i:matrix:solubilizers:sorbefacients:additives=1:1-3000:0-165:0-80:0.001-260, wherein the effective quantity is equivalent to 1.25-400mg of the PDE-5i, and the weight of each unit preparation is 0.8-4 grams. Through rectal administration, the rectal administration composite can not only overcome the defects of poor systematic administration treatment effect, high toxic and side effects, irregular absorption, low bioavailability, and the like of oral preparations, and the like, but also shorten the effectual time of pharmaceuticals, prolong the action time of the pharmaceuticals, promote the release and the absorption of the pharmaceuticals and enhance ten efficiency of the pharmaceuticals reaching a target organ, thereby providing better treatment means for medical personnel and patients; and in addition, the invention has simple production process and is suitable for industrialized batch production.
US20120087869 Methods for distributing agents to areas of brain Broad cerebrospinal fluid (CSF) distribution of an agent is achievable by delivering the agent in a liquid formulation to the CSF at flow rates less than 500 microliters per hour, such as between about 2 microliters per hour and about 100 microliters per hour.
EP1513482A2 Topical use of at least one double-stranded rna oligonucleotide (ds rna) The invention relates to a novel use of at least one double-stranded RNA oligonucleotide (ds RNA) for a topical application and topical compositions comprising at least one double-stranded RNA oligonucleotide encapsulated within a physiologically-acceptable medium. The invention further relates to a cosmetic treatment method using at least one double-stranded RNA oligonucleotide.
EP2259800A1 Use of pyrimidine derivatives for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members The present invention relates to the use of compounds of formula (I),in the treatment of Epidermal Growth Factor Receptor (EGFR) family members dependent diseases or diseases that have acquired resistance to agents that target EGFR family members, use of said compounds for the manufacture of pharmaceutical compositions for the treatment of said diseases, combinations of said compounds with EGFR modulators for said use, methods of treating said diseases with said compounds and pharmaceutical preparations for the treatment of said diseases comprising said compounds alone or in combination, especially with an EGFR modulator.
WO2014043866A1 Thiophene [2, 3-d] pyrimidine derivative, and preparation method and use thereof Provided are a thiophene [2, 3-d] pyrimidine derivative containing isoxazole heterocycle as represented by formula (I), or pharmaceutically acceptable salt thereof, as well as preparation methods, uses and pharmaceutical compositions thereof. The compounds can be used to treat diseases such as tumor, cancer and the like.
US20080033060 Use Of A Compound Modulating At Least One Receiver Selected In A Group Comprising An Interleukin 8 Type B Receptor And Pacap-1 Receptor For Porparing A Pharmaceutical Composition For Rosacea Treatment The invention relates to the use of a modulator of at least one receptor chosen from the group comprising the IL-8RB receptor and the PAC-1 receptor for the preparation of a pharmaceutical composition for treating rosacea.
CN103333216A 5alpha-6-ketone-cholestane analogue and applications thereof The invention discloses an 5alpha-6-ketone-cholestane analogue and applications thereof. The structure general formula of the 5alpha-6-ketone-cholestane analogue is . The analogue has therapeutical effects on central nervous system diseases, which is related with that the analogue can be used as steroid nerve anti-inflammatory preparations. The analogue has no obvious cytotoxicity, can reduce the area of cerebral hemorrhage effectively, and has good application prospects in preparation of new-type medicaments treating central nervous system diseases.
US20090263353 Novel Sulphonylpyrroles as Inhibitors of Hdac S Novel Sulphonylpyrroles Compounds of a certain formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.
WO2014045029A1 2-(2-aminocyclohexyl)amino-pyrimidine-5-carboxamides as spleen tyrosine kinasei(syk) inhibitors The present invention relates to compounds of formula (Ia), (Ib) or (Ic): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma, COPD, allergic rhinitis, chronic sinusitis, atopic dermatitis, psoriasis, rosacea, alopecia, allergic conjunctivitis and dry eye disease
WO2006046007A1 The treatment of inflammatory bowel disease Actarit or a salt thereof is useful for the treatment of inflammatory bowel disease.
US20090264336 glucokinase activator 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide or a salt ; deprotecting silanol group with an acid; type 2 diabetes Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
US20050101588 7-Amino alkylidenyl-heterocyclic quinolones and naphthyridones The present invention relates to compounds having a structure according to Formula I wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.
WO2005000789A1 2-amino-3-alkoxybicyclo[3.1.0]hexane derivative A drug which is effective in treatments for and prevention of schizophrenia, anxiety, and diseases related to these, i.e., psychiatrical disorders such as depression, bipolar disorder, and epilepsy. The drug has an antagonistic effect on a Group II metabotropic glutamate receptor. It is a 2-amino-3-alkoxybicyclo[3.1.0]hexane-2,6dicarboxylic acid derivative represented by the formula [I]: [I] (wherein R1 and R2 are the same or different and each represents hydrogen, C1-10 alkyl, etc.; and R3 represents naphthyl or phenyl substituted by one to five substituents selected from the group consisting of cyano, phenyl, and halogeno and R4 represents hydrogen, C1-10 alkyl, etc., or R3 and R4 each represents phenyl), a pharmaceutically acceptable salt of the derivative, or a hydrate of either.
US8486948 Piperazinodihydrothienopyrimidine derivatives The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2, preferably however SO, and wherein R3, R4, R4′, R5, R6 and R7 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers.
US20080175922 Topically treating eye disorders, diseases and inflammation without sensitivity Provided are ophthalmic pharmaceutical compositions comprising gallium. These compositions are designed primarily for topical ocular and intraocular administration. Also provided are methods of use for the compositions in the treatment of human and veterinary diseases and disorders. Treatable diseases and disorders include adverse conditions of the eye and adnexal tissues of the eye. These adverse conditions comprise inflammatory conditions, infections, cancers, and other pathological conditions.
EP1525030A1 Combination of an allosteric alkyne inhibitor of matrix metalloproteinase-13 with a selective inhibitor of cyclooxygenase-2 that is not celecoxib or valdecoxib The invention provides a combination, comprising an allosteric alkyne inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with a selective inhibitor of COX-2, or a pharmaceutically acceptable salt thereof, that is not celecoxib or valdecoxib. This invention also provides a method of treating a disease that is responsive to inhibition of MMP-13 and cyclooxygenase-2, comprising administering to a patient suffering from such a disease the invention combination comprising an allosteric alkyne inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with a selective inhibitor of COX-2, or a pharmaceutically acceptable salt thereof, that is not celecoxib or valdecoxib. This invention also provides a pharmaceutical composition, comprising the invention combination comprising an allosteric alkyne inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with a selective inhibitor of COX-2, or a pharmaceutically acceptable salt thereof, that is not celecoxib or valdecoxib, and a pharmaceutically acceptable carrier, diluent, or excipient. This invention also provides a combination comprising an NSAID, or a pharmaceutically acceptable salt thereof, and an allosteric alkyne inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof. This invention also provides a pharmaceutical composition, comprising the invention combination comprising an allosteric alkyne inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with an NSAID, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. This invention also provides a method of treating a disease that is responsive to inhibition of MMP-13 and cyclooxygenase 1 or cyclooxygenase-2, comprising administering to a patient suffering from such a disease the invention combination comprising an allosteric alkyne inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with an NSAID, or a pharmaceutically acceptable salt thereof. The invention combinations may also be further combined with other pharmaceutical agents depending on the disease being treated.
WO2009151057A1 Process for production of antioxidant active substance Disclosed is a process for producing carnosic acid (the major antioxidant active substance contained in a rosemary plant) with high efficiency by carrying out the ortho-position oxidation of a phenol with an oxidizing agent (e.g., 2-iodoxybenzoic acid) and the subsequent ester removal reaction by using, as a starting material, pisiferic acid (the main component of Chamaecyparis pisifera which is a plant which has been planted in great numbers as wood resources). Specifically disclosed is a process for producing an antioxidant active substance contained in a rosemary plant and represented by general formula (5). The process is characterized by comprising: a first step of oxidizing a pisiferic acid derivative represented by general formula (1) with an oxidizing agent represented by general formula (2) or (4); and a second step of reducing or hydrolyzing a pisiferic acid derivative intermediate produced in the first step.
WO2008002602A1 Use of n-desmethylclozapine to treat psychosis Disclosed herein is are methods to treat neuropsychiatric diseases including psychosis. Treatment is carried out by administering a therapeutically effective amount of N-desmethylclozapine to a patient suffering from a neuropsychiatric disease.
WO2014083567A8 Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors A method of preventing tumor metastasis with the proviso that the tumor is not glioma is provided. The method comprising administering to a subject in need thereof a therapeutically effective amount of an inhibitor of synaptojanin 2 (SYNJ2), thereby preventing tumor metastasis. Also, provided is a method of treating cancer. The method comprising, administering to a subject in need thereof a therapeutically effective amount of an inhibitor of synaptojanin 2 (SYNJ2) and an inhibitor of a cell surface receptor associated with an onset or progression of cancer, thereby treating cancer.
US20080108642 Matrine, oxymatrine, and sinomenine (hydrochloride); rheumatoid arthritis and cancer The present invention relates to a composition as effective constituent of a medicine having anti-angiogenesis synergy effect and belongs to the field of medicine compositions. The recipe is composed of matrine and sinomenine hydrochloride with a content ratio of matrine:sinomenine hydrochloride=1:0.05 to 1. The recipe of the present invention has synergic actions of efficacy enhancing and toxicity reducing, has obvious therapy effect to angiogenesis-related diseases such as rheumatoid arthritis and cancer, has clear base of medicine effective substance, and maintain the characteristic of traditional Chinese medicine of recipe association.
US20120114639 Compositions and methods for inhibiting viral and/or bacterial infections We describe herein compositions and methods related to inferring with microbial infection. Generally, the compositions include an infection antagonist that inhibits formation of a heparin sulfonated proteoglycan (HSPG)-containing infection complex. Generally, the methods include administering to a subject an amount of a composition as described herein effective to inhibit infection by a microorganism that that infects a host through interactions that involve HSPG.
CN1785193A Amino acid (-) ofloxacin water soluble salt A water-soluble salt of amino acid (-) ofloxacin with high solubility and antibacterial effect has a molecular formula C18H20FN3O4 A*nH2O is prepared from the semi-hydrated (-) of loxacin (C18H20FN3O4/2H2O) and aspartic acid or glutamic acid through dissolving in water, adding it to alcohol, educing out white crystals, and drying.
US20120239007 Implantable Devices and Methods for Treatment of Pain by Delivery of Fentanyl and Fentanyl Congeners The invention features devices and methods for treatment of pain. The drug delivery device is a drug delivery system adapted for whole implantation in a subject and to provide pain relief by delivery of fentanyl or a fentanyl congener (e.g., sufentanil) over a protracted period of time (e.g., at least 3 days or more than 3 days). The device comprises a housing defining a reservoir that contains a drug formulation, a pump operatively connected to the housing so as to facilitate movement of drug out of the reservoir and out of the device, and a thermal expansion element which defines a flow pathway comprising a thermal expansion channel to accommodate thermal expansion of formulation in the reservoir. The device can further comprise a valve positioned within the flow pathway so as to prevent movement of drug out of the reservoir prior to use.
EP1131310B1 Chrystals of 5- 6-(2-fluorobenzyl)oxy-2-naphthyl methyl]-2,4-thiazolidinedione The invention relates to type A crystal of 5-[{6-(2-fluorobenzyl)oxy-2-naphthyl}methyl]-2,4-thiazolidinedione characterized to have characteristic absorption peaks (2υ) at 11.5°±0.3°, 14.5°±0.2°, 16.2°±0.3°, 17.0°±0.3°, 17.7°±0.2°, 18.6°±0.3°, 19.1°±0.2°, 21.3°±0.4°, 22.4°±0.5°, 25.7°±0.5° and 28.3°±0.5° in a powder X-ray diffraction pattern, and also to a method for preparation thereof, and a pharmaceutical composition comprising the same. The crystal is excellent in stability, and has advantages in handling, storage, and pharmaceutical preparation. The invention also relates to type B, C and D crystals of said compound.
CN102659800A Hypoxia-activated antitumor compounds and application thereof The invention relates to the field of medicinal chemistry, and in particular relates to hypoxia-activated antitumor compounds (I) or (II) and application thereof. Pharmacological experiments prove that the compounds have excellent cytotoxic activity and hypoxia selectivity and can be prepared into antitumor medicaments.
US20120183634 Synergistic Compositions That Treat or Inhibit Pathological Conditions Associated With Inflammatory Response A natural formulation of compounds that would to modulate inflammation is disclosed. The formulation would also inhibit expression of COX-2, inhibit synthesis of prostaglandins selectively in target cells, and inhibit inflammatory response selectively in target cells. The compositions containing at least one fraction isolated or derived from hops. Other embodiments relate to combinations of components, including at least one fraction isolated or derived from hops, tryptanthrin and conjugates thereof, rosemary, an extract or compound derived from rosemary, a triterpene species, or a diterpene lactone or derivatives or conjugates thereof.
US20080145453 4-(piperimidine-2thione)phenyl derivatives; kinesin Eg5 inhibitor; anticarcinogenic agent; the aldehyde, the ketone and the thiourea are reacted together in the solid phase, grafted onto resin by esterification, and detached by hydrolysis The invention concerns molecules of formula (I), drugs containing same and their use as anti-cancer agents.
WO2013063679A1 Use of neul sialidase inhibitors in the treatment of cancer Use of Neul sialidase inhibitors for the treatment of cancer as a monotherapy or in combination with known chemotherapeutics. Preferably, Neul sialidase inhibitors are oseltamivir phosphate or 2-deoxy-2,3-dehydro-N-acetylneuraminic acid (DANA) or analogues thereof.
EP1711184B1 (3-oxo-3,4-dihydro-quinoxalin-2-yl-amino)-benzamide derivatives and related compounds as glycogen phosphorylase inhibitors for the treatment of diabetes and obesity The invention features pharmaceutically active quinoxalinones of formula (1), compositions containing them, and methods of making and using theme: Formula (I) wherein R1 is H, C 1-6 alkyl, or halo; R2 is H or halo; R3 is H, C 1-6 alkyl, X is N or CH; Y is a covalent bond, -NHCO- or -CONH-; Z is phenyl or a 5 or 6-membered heterocyclyl with between l and 2 heteroatoms independently selected from N, O, and S; and n is 0, 1 or 2; or a pharmaceutically acceptable salt, ester, amide, hydrate, or solvate thereof; as well as their use as glycogen phosphorylase inhibitors for the treatment of i diabetes and obesity.
US8012926 Amino acid composition and supplementary liquid containing the same An amino acid composition comprises alanine, arginine, aspartic acid, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine, valine, and glutamine. The amino acid composition of the present invention has such an effect that it can improve the action of promoting the process wherein the body fat is converted into the energy required for the physical exercise during and/or after the anoxic motions performed under an extremely high load.
CN101693073B Compound caesalpinia pulcherrima spraying agent and preparation method thereof The present invention relates to a compound caesalpinia pulcherrima aerosol and a preparation method thereof. The compound caesalpinia pulcherrima aerosol is made of crude drug fresh impatiens noli-tangere, safflower, borneol, resina draconis, frankincense, myrrh and propellent. Compared with the compound caesalpinia pulcherrima liniment, the compound caesalpinia pulcherrima aerosol has less impurity and higher content of effective components, does not irritate the skin, and is better in the effects of detumescence and analgesia as well as invigorating the circulation of blood.
US7687638 C-(3-Methyl-5-phenyl-3H-benzoimidazol-4-yl)-methylamine; diabetes, fasting plasma glucose (IFG), metabolic acidosis, ketosis, appetite regulation, obesity, immunosuppressants or cytokine release regulation, autoimmune diseases such as inflammatory bowel disease, multiple sclerosis and arthritis Compounds, pharmaceutical compositions, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound of the formula: wherein the substituents are as defined herein.
CN101428013A Uses of tanshinone IIA vein emulsion in treating brain diseases The invention relates to application of tanshinone II A venous emulsion in treatment of brain disease. After intravenous injection of tanshinone II A venous emulsion or venoclysis thereof after being diluted by other injection into the body of a patient, the tanshinone II A venous emulsion can rapidly permeate the blood brain barrier, therefore the invention can be used for treating ischemic cerebrovascular diseases, hemorrhagic cerebrovascular diseases and brain tumor.
US8138224 Nutritional or therapeutic composition containing the compound oleuropeine or one of the derivatives thereof The present invention provides a nutritional composition and a pharmaceutical composition to be used for humans or animals comprising as active compound the oleuropein compound or one derivative thereof.
EP2606896A1 Sterile emulsion containing hyaluronate and glucocorticoid, and use of such emulsion in the treatment of inflammatory joint disorders The invention relates to a sterile emulsion comprising 80-99.9 wt.% of a continuous aqueous phase and 0.01-20 wt.% of a dispersed lipid phase, wherein the emulsion contains 0.1-10% of hyaluronate by weight of said aqueous phase; and 0.01-50% of a lipophilic glucocorticoid by weight of said lipid phase. This emulsion can suitably be administered intra-articularly to patients suffering from an inflammatory joint disorder to maintain mobility of the joint and to provide effective relief for intra-articular pain and inflammation. The emulsion offers the advantage that following intra-articular administration it is effective for a prolonged period of time.
CA2173974C Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having formula (I), and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8-positions of the quinoxaline nucleus, and R3, R4 and R5 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, reduction of at least one effect of an inflammatory disorder, increase in renal fluid flow, and alteration in the rate of fluid transport in the gastrointestinal tract.
US20110206779 Gastric ulcer therapeutic agent A gastric ulcer therapeutic agent comprising as an active ingredient a composite hydroxide of a hydrotalcite and an aluminum hydroxide compound, which composite hydroxide is represented by the formula (1), Mg1-xAlx(OH)2-ny(An-)y/n (H2O)m (1) wherein An- represents an anion, n represents a valence of the anion in the range of 1 to 4, x is in the range of 0.34, R<7> or R<8> is and X, Y, R<1> to R<13> and n are as defined in the description, and all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPARdelta and/or PPARalpha agonists.
US20100286280 Inhibitors of eppin/semenogelin binding as male contraceptives Compounds suitable for use in providing male contraception, an assay method for identifying such compounds, and methods of providing contraception using the compounds, are provided. The compounds described herein inhibit Eppin-semenogelin binding, and inhibit forward motility of sperm in humans and other primates. The assays identify compounds which both inhibit eppin-semenogelin binding and inhibit sperm motility, and can be carried out in a high throughput manner, using labeled recombinant Eppin and semenogelin. The compounds can be used in oral or transdermal compositions to temporarily and reversibly inhibit male fertility. They can also be used in addition to, or in place of, spermicides in spermicidal compositions, such as those used in conjunction with condoms, diaphragms, and spermicidal jellies.
US8741303 Immunogenic LHRH compositions and methods relating thereto The present invention relates generally to an immunogenic LHRH composition and more particularly to an immunogenic LHRH composition comprising a LHRH C-terminal fragment of at least five amino acids. The present invention is useful, inter alia, as a prophylactic and/or therapeutic agent for the modification of fertility and behavior patterns of animals, the achievement of livestock production gains such as increasing growth, decreasing feed conversion ratios or the control of unwanted organoleptic characteristics or the treatment of disorders of the reproductive organs.
CN102949298A Application of usnic acid and/or salts thereof The invention discloses an application of usnic acid and/or salts thereof as a propionibacterium acnes inhibitor. The invention further discloses an application of usnic acid and/or salts thereof in preparation of drugs or cosmetics for preventing or treating pimples caused by the breeding of the propionibacterium acnes. The invention can effectively treat the pimple generation caused by the breeding of the propionibacterium acnes. The usnic acid and/or salts thereof are from both the sunglow plants and the artificial synthesis, have the advantages of low toxicity for the human body and high bacteriostatic action for the propionibacterium acnes, can be prepared into various external medicine dosage forms and cosmetics and have good application prospects.
CN102204927A Medicament for treating endoplasmic reticulum (ER) breast cancer The invention discloses a medicament for treating endoplasmic reticulum (ER) breast cancer and belongs to the technical field of pharmacy. The active ingredients of the medicament are arsenic trioxide and tamoxifen. Experiments show that after being used together, the arsenic trioxide and the tamoxifen have obvious effect. To inoculated BALB/c-nu female nude mice, the tumor volume inhibition ratio of the composite medicament is up to 77.42 percent and the tumor weight inhibition ratio of the medicament is up to 76.28 percent. In addition, the formulation of the medicament is also improved, namely the arsenic trioxide is wrapped through collagen and then is mixed with the tamoxifen; and after a proper amount of diluent is added into the mixture, the mixture is prepared into oral formulations, such as powder, pills or capsules and the like. A normally used food component, namely water-soluble collagen, serves as a carrier and has high entrapment efficiency to the arsenic trioxide; the in-vivo retaining time of the arsenic trioxide can be prolonged while the side effect of the arsenic trioxide on gastrointestinal tract is reduced; long-time effective blood concentration is maintained; and while the effect of the medicament is maintained, great convenience is brought to patients and the injection pains of the patients are relieved.
CN102391272A 1,4-disubstituent-1,4-dihydrobenzopranyl [4,3-c] pyrazole compounds The invention discloses 1,4-disubstituent-1,4-dihydrobenzopranyl [4,3-c] pyrazole compounds and a preparation method and application thereof. The preparation method comprises the following steps of: previously preparing a Vilsmeier reagent by using di (trichloromethyl) carbonate and N,N-dimethyl formamide as raw materials, adding a flavanone compound I into the Vilsmeier reagent, obtaining a flavanone-4-chloro-3-formyl compound II by chlorination formylation reaction, condensing the obtained flavanone-4-chloro-3-formyl compound and a substituted phenylhydrazine hydrochloride to obtain a flavanone-4-chloro-3-phenylhydrazone compound III, performing cyclization on the phenylhydrazone compound III under the action of sodium hydride, and thus obtaining target compounds IV. The 1,4-disubstituent-1,4-dihydrobenzopranyl [4,3-c] pyrazole compounds have in vitro inhibiting effect on tumor cell strains, wherein the compound IVb and IVf have remarkable in vitro inhibiting effect on human leukemia cell strains HL60.
CN101787030A Preparation and application methods of anti-HIV compound, morus ignin L The invention discloses preparation and application methods of an anti-HIV compound, morus ignin L. The preparation method is characterized by taking dry cortex mori, extracting the dry cortex mori with water or a water-soluble organic solvent; and combining extract, filtering the extract, carrying out extraction separation on the filtrate with organic solvent, concentrating the extracts at reduced pressure and separating and purifying the extracts by a chromatographic process, thus obtaining the morus ignin L. The application method is characterized by adding drug carriers into the morus ignin L with anti-HIV activity, carrying out mixing, granulating and drying and then preparing the morus ignin L and the drug carriers into granules, capsules, tablets, oral liquid or injection according to the common preparation method of the drugs; or adding the carriers and preparing the carriers and the morus ignin L into health drinks or health food according to the conventional method. Experiments prove that the inhibition ratio of the morus ignin L with anti-HIV activity on the HIV-LTR sequence activity can reach over 95% and can be used for preparing anti-HIV drugs. The methods are simple and practicable and are suitable for popularization and application.
WO2012144080A1 Skin barrier function improving agent The purpose of the present invention is to provide a novel TRPV receptor activator which is suitable for the improvement in a skin barrier function. The purpose can be achieved by providing a TRPV receptor activator which comprises at least one compound selected from compounds respectively represented by the formulae or a plant extract containing the at least one compound in an effective amount for acting as a TRPV receptor activator. (In the formulae, a hydroxy group may be substituted by a methoxy group or an ethoxy group; and a methoxy group may be substituted by a hydroxy group or an ethoxy group.)
WO2007017092A1 Substituted 4-benzyloxy-benzoic acid amide derivatives The present invention relates to novel substituted 4-benzyloxy-benzoic acid amide derivatives, processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol Receptor 1 (CMR-1) activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
US8426418 Method to treat melanoma in BRAF inhibitor-resistant subjects Methods to treat cancer patients, especially melanoma patients, who have BRAF mutations and have become resistant to BRAF mutant kinase inhibitors employ inhibitors of multiple receptor tyrosine kinases. In addition, methods are described for identifying pharmaceutical compositions and drugs that will be successful in treating these patients.
US20110166182 Selective Estrogen Receptor Modulator for the Treatment of Osteoarthritis The present invention is directed to a compound of the formula (A): or a pharmaceutically acceptable salt thereof; and also to compounds of formula (I): or a pharmaceutically acceptable salt thereof.
CN101797277A Method for detecting Jingan capsule The invention discloses a method for detecting a capsule for treating cold. The capsule is prepared from honeysuckle, common andrographis herb, isatis root, dandelion, acetaminophen, amantadinehydrochloride and chlorphenamine maleate. The invention increases the content detection of the amantadinehydrochloride, the honeysuckle and the dandelion on the basis of the traditional quality standard, improves a content detecting method of the acetaminophen, can carry out more effective control on main medicament components of a Jingan capsule, and enables the quality monitoring level of the Jingan capsule to be greatly improved. The application of the invention is more beneficial to manufacturers and the supervisory management department to monitor the product quality and can provide better guarantee for the medical department and the treatment of patients.
US20100292166 PHARMACEUTICAL COMPOSITION FOR TREATING MALIGNANT TUMORS CONTAINING HUMAN p31 GENES A pharmaceutical composition for the treatment of malignant tumors comprising a human p31comet gene encoding protein represented by SEQ ID NO: 3 or 4 as an effective component is provided. The pharmaceutical composition can suppress cancer cell growth, induce apoptosis and kill cells by overexpressing p31comet in the solid malignant tumor cells. Therefore, the pharmaceutical composition can be effectively used for gene therapy.
CN102488685A Application method of liposome preparation containing compound amino acid component The invention discloses an application method of a liposome preparation containing a compound amino acid component. The method utilizes the liposome preparation containing the compound amino acid component prepared by patent application 201110442862.6 to prepare a product that can be directly applied to various acute and chronic wounds; and an application product of the liposome preparation containing the compound amino acid component is prepared by filling 1-500 g of the preparation into each aluminium pipe, plastic-aluminum pipe or plastic tubing, carrying out end-capping and carrying out radicidation by cobalt-60. The preparation prepared by a special liposome technology and a film forming technology can be applied to wound and has the following advantages: a layer of film can be formed on the wound after coating in a short time, and the film can provide a semi-hermetic, moistening and ventilating environment to facilitate wound healing; and the liposome loading cell growth factorslike amino acid enters into wound cells directly, through modes of adsorption and fusion, to participate metabolism of the cells and promote growth and creep of cells, so as to promote wound healing and shorten a time for wound healing.
US20110144145 Methods for treating visceral fat conditions Disclosed are methods and compositions for treating visceral fat conditions and/or metabolic syndrome using combinations of naltrexone and bupropion.
US20120041074 Method of inducing neovascularization A method for inducing neovascularization in which a pharmaceutically effective amount of polyethylene glycol (PEG) is injected into the tissue of the subject for purposes of accelerating wound healing and mimicking age related macular degeneration, cancer, tumors, and atherosclerosis for further research purposes.
CN101801393A Antiviral colloidal silver composition A colorless composition comprising silver particles and water is disclosed. The particles have an interior of elemental silver and an exterior of ionic silver oxide, wherein the silver particles are present in the water at a level of about 5-40 ppm. The composition manifests significant antiviral properties and is effective against avian influenza virus. Methods of use of the composition are described.
US20050267153 Administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds alone or in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents; inhibiting replication and secretion, reduced toxicity Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds alone or in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds alone or in combination with nucleoside antiviral agents, nucleotide antiviral agents, or mixtures thereof, and immunomodulating/immuno-stimulating agents.
CN201642568U Meridian therapeutic band for internal medicine in hospital The utility model relates to a meridian therapeutic band for internal medicine in a hospital, which comprises a base band, a Chinese medical patch and four magnetic powder strips. The base band is a basic band, the whole structure of the base band is of a rectangular shape, the four sides of the base band respectively adopt a bonding adhesive tape near the edges thereof, the Chinese medical patch is arranged in the middle of the base band, and the four magnetic powder strips are vertically arranged on the Chinese medical patch. The Chinese medical patch is prepared with 2g of galangal, 3g of Chinese mugwort leaf, 1g of elecampane, 1g of cinnamon, 1g of fructus amomi, 3g of flos caryophylli, 2g of rhizoma sparganii, 3g of curcuma zedoary, 4g of safflower and 3g of magnetite. The preparation of the Chinese medical patch comprises the following steps: grinding the raw materials into powder, preparing an ointment according to the adhesive plaster process, and spreading the ointment in the middle of the base band, thereby obtaining the Chinese medical patch. The four magnetic powder strips are arranged between the Chinese medical patch and the base band. The utility model has the advantages of simple overall structure and convenient operation and use. When the internal medical patient suffers from the pain for unknown reasons, the utility model can be applied on the navel of the patient for treatment, with the central magnetic powder strips aligned with the two sides of the navel.
US20070015830 Use of a retinoid type compound to modulate in vivo the decoupling activity of the protein UCP2 The invention relates to the use of a compound of the retinoid type particularly retinoid acid for the preparation of a medicament capable of modulating in vivo the decoupling activity of decoupling proteins. These compounds can be used conveniently for the treatment of diseases associated to an increase or reduction of the activity of decoupling proteins. According to a preferred embodiment, the retinoid acid will be used for the treatment of disease associate to a reduction of the decoupling activity of the protein UCP2 such as for example obesity.
CN102133218B Ceforanide composition The invention belongs to the technical field of medicine, and in particular relates to a ceforanide composition. The medicinal composition contains 100 to 1,000 weight parts of ceforanide and 20 to 500 weight parts of arginine.
WO2014001183A1 Pharmaceutical composition having synergistic action of direct catalase inhibitors and modulators of no metabolism or of extracellular superoxide anion production which lead to catalase destruction The present patent application relates to a pharmaceutical composition, characterized in that it comprises at least one active ingredient which can bring about a singlet oxygen-independent direct catalase inactivation, and in that the composition further comprises at least one active ingredient which leads to inactivation of catalase as a result of modulation of the nitrogen oxide or superoxide anion metabolism of the cells and subsequent singlet oxygen formation.
US20120264680 Regulation of energy metabolism and obesity by modulating b cell activating factor (baff, blys) or baff signaling Provided herein are methods and compositions for modulating energy metabolism and weight in mammals, in particular by modulating thermogenesis associated with brown fat, including thermogenesis by brown fat or brown fat cells, adaptive thermogenesis by brown fat or brown fat cells, thermogenic capacity of brown fat or brown fat cells, or a combination thereof. More specifically, methods and compositions provided herein for treating or preventing obesity, or methods and compositions for identifying compounds effective for treating or preventing obesity are taught in connection with ligands such as B-cell activating factor (BAFF) and a proliferation-inducing ligand (APRIL), their receptors, and molecules that modulate the interactions between the ligands and receptors.
US20090036488 Recurrence preventive therapeutic agent for psychostimulant-induced psychosis and schizophrenia The present invention provides a therapeutic agent for preventing recurrence of psychostimulant-induced psychosis and schizophrenia. This therapeutic agent for preventing recurrence of psychostimulant-induced psychosis and schizophrenia includes a drug that amplifies serotonin signals as an active component. This therapeutic agent for preventing recurrence of psychostimulant-induced psychosis and schizophrenia includes a drug that amplifies serotonin signals as an active component. This therapeutic agent for preventing recurrence of psychostimulant-induced psychosis and schizophrenia includes a drug that amplifies serotonin signals as an active component.
WO2012084446A1 Compound having antibacterial activity It is described the use of betamethasone as antibacterial agent.
EP1958666A1 Heterocyclic-substituted alkanamides as therapeutic compounds Use of compounds of the general formula (I) and pharmaceutically acceptable salt thereof, in which R1 and R2 have the definitions illustrated in detail in the description, as beta-secretase, cathepsin D, plasmepsin II and/or HIV protease inhibitors.
US6943026 A mixture of first and second nucleic acid constructs, is used for gene therapy, as antitumor agents, antiproliferative agents, suppressed by a wild-type p53 allele in non-tumour cells relative to tumor cells, prodrug activating thymidine kinase Compositions for targeting expression of a gene such as an antitumor gene may contain a first nucleic acid construct in which expression of a first gene is controlled by a first promoter whose function is suppressed in non-tumor cells, and a second nucleic acid construct in which expression of a second gene for down-regulating the first gene in non-tumor cells is controlled by a second promoter that is up-regulated in non-tumor cells. The second promoter may be regulated by means of p53 binding, targeting expression of the first gene to cells in which p53 down-regulation of expression is disrupted, e.g. cells in which p53 is mutated. The first promoter may be one which is unregulated in tumor cells, for example the Hsp70 promoter which is upregulated in mutant p53 tumor cells. A suitable antitumor agent in thymidine kinase.
CN103480001A Acupoint massaging assisting preparation, preparation technology and application of preparation technology The invention relates to an acupoint massaging assisting preparation which is characterized by comprising a basic reagent and a free-radical scavenger. 10 parts of basic reagent and 0.5-0.001 part of free-radical scavenger are mixed based on the weight ratio. The acupoint massaging assisting preparation, a preparation technology and application of the preparation technology can achieve good effects of moistening, pushing, expanding and massaging, eliminate pain and discomfort of all parts of the human body in a short period in the assisted massaging process, and effectively remove free radicals of acupoints.
CN103570705A Substituted N-((1', 3'-azole-4'-yl)-methyl)-4-benzoyl-hexahydropyridine compound and applications thereof The invention discloses a substituted N-((1', 3'-azole-4'-yl)-methyl)-4-benzoyl-hexahydropyridine compound represented by formula I, a preparation method thereof, and applications of the substituted N-((1', 3'-oxazole-4'-yl)-methyl)-4-benzoyl-hexahydropyridine compound in preparation of antituberculous drugs. The substituted N-((1', 3'-azole-4'-yl)-methyl)-4-benzoyl-hexahydropyridine compound possesses activity on mycobacterium tuberculosis-susceptible strains, and also possesses activity on strains with tolerance on traditional first-line antituberculous drugs such as isoniazide and rifampicin, and is a novel mycobacterium tuberculosis resistant compound with a promising application prospect.
CN103462956A Application of Nardoaristolones A in preparation of medicaments for increasing erythrocytes The invention relates to new application of compound Nardoaristolones A in the field of pharmacy. The invention discovers that Nardoaristolones A can increase erythrocytes, so that Nardoaristolones A can be used for preparing the medicaments for treating low erythrocytes, has high activity, has prominent substantive features, and has significant progress.
US20100093692 Piperidinyl-piperidine and piperazinyl-piperidine for use in the treatment of diabetes or pain The present invention relates to Compounds of Formula (I), compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IFG) in a patient.
CN103435611A Multi-target point alpha-pyridoin compounds and preparation method and application thereof The invention discloses multi-target point alpha-pyridoin compounds, having a structural general formula shown in the specification. The multi-target point alpha-pyridoin compounds have good inhibiting and killing effects on various pathogenic bacteria; and a part of compounds have higher bacteriostatic activity than positive controls such as penicillin G, kalamycin and ketoconazole, can be used for preparing anti-injection drugs. The invention further discloses a preparation method of the multi-target point alpha-pyridoin compounds.
CN100998599A Compound terbinafine and root of large flowered skullcap cream and its preparing method A terbinafine-scutellaria cream for treating dermatitis, eczema, ringworm of body, tinea manuum, tinea pedis, itching, etc is prepared proportionally from terbinafine hydrochloride, neomycin sulfate, triamcinolone acetonide acetate, the extracts of scutellaria root and dittany bark, and O/W-type cream matrix. Its preparing process is also disclosed.
EP2301922A1 Pyridone compound [Problems] A useful compound which can be used as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease is provided. [Means for Solution] The present inventors have conducted extensive studies on EP4 receptor agonists, and as a result, have found that a novel pyridone compound, in which a group having an acidic group is substituted at the 1-position of the pyridone ring, the 6-position is bonded with an aromatic ring group via a linking part, and the linking part contains a nitrogen atom, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action, it is useful as a pharmaceutical, in particular, as an agent for treating peripheral arterial occlusive disease.
WO2011137759A1 Novel ecdysterone synthesis derivative, preparation method and use thereof A compound having the structure of formula (I), pharmaceutically acceptable salts or solvates thereof are disclosed. A preparation method of the said compound, a pharmaceutical composition containing it and use thereof in the manufacture of hypoglycemic medicaments are also disclosed.
WO2012135027A2 Thiolactone antibiotics This invention provides a compound having the structure (I) wherein R1 is H, (II) or (III), wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is (IV), (V), (VI), (VII), (VIII), or (IX), wherein m is an integer from 0 to 8; R3 is an amino, alkyl, aryl, heteroaryl, diol, piperazine, morpholine, piperidine, triazole, azide or biphenyl, each with or without substitution, branched or unbranched, or (X); and R4 is alkyl, aryl, or heteroaryl, each with or without substitution, branched or unbranched, R2 is H, CH3, or alkyl, aryl, heteroaryl, pyrrole, diazole, or triazole, each with or without substitution, branched or unbranched, or (XI), wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is (IV), (V), (VI), (VII), or (VIII); and R6 is azide, methoxy, trifluoromethyl, biphenyl, substituted phenyl, substituted triazole, or alkyl, aryl or heteroaryl, with or without substitution, branched or unbranched, when R1 is H then R2 is other than H or CH3, and when R2 is H or CH3 then R1 is other than H, or a pharmaceutically acceptable salt thereof.
US20100179218 Oculoselective drugs and prodrugs Compounds of the following formula are disclosed: Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions are disclosed.
US20050152999 supercritically extracting an herb to obtain an oil extract and a residue;extracting the residue in a water/alcohol liquid mixture to obtain a post-supercritical hydroalcoholic extract; evaporating the water/alcohol liquid to form a powdered extract; mixing the powdered extract with the oil extract. A method is provided for effecting smoke detoxification in a human by using a composition that is made of effective amounts of supercritical extract and hydroalcoholic extract of turmeric.
WO2006063033A2 Aryl amide sphingosine 1-phosphate analogs The present invention provides compounds that have antagonist activity at the S1P1 and/or S1P3 receptors. These compounds have enhanced selectivity and potency at the S1P1 and/or S1P3 receptors.
WO2009079768A1 Methods of inhibiting tumor growth using ttk antagonists The present invention relates to methods for treating TTK positive breast cancers or soft-tissue sarcomas in a mammalian subject by administering a therapeutically effective amount of a TTK antagonist. The invention also provides compositions comprising a TTK antagonist and a HER-2 antagonist, as well as methods of diagnosing a basal-like breast cancer and methods of determining the prognosis of a subject having a cancer by assessing expression of TTK in a tumor sample from a subject.
US20100056626 Cosmetic product for the treatment of cicatricial tissues A method for cosmetic treatment of cicatricial tissues comprising the step of applying to the cicatricial tissue a cosmetic product which contains one or more cyanoacrylates.
CN101397326A Ginsenoside Rb1 containing impurity ginsenoside Rg2 The invention discloses a standard ginsenoside Rb1 effective constituent, comprising the ginsenoside Rb1 with more than 90 percent and less than 100 percent of content. The effective constituent is characterized in that the content of impure ginsenoside Rg2 is larger than 0 and smaller than 3 percent, or the content of impure ginsenoside Rg2 is equal to or larger than 0.01 percent and smaller than 3 percent, or the content of impure ginsenoside Rg2 is equal to or larger than 0.01 percent and equal to or smaller than 1 percent, or the content of impure ginsenoside Rg2 is equal to or larger than 0.01 percent and equal to or smaller than 0.5 percent. Pharmacological test proves that, the standard effective constituent of the application has great pharmacological function, which can be prepared into pharmaceutically medicinal preparation.
US20120077873 Methods of Reducing Blood Lactate Concentration The present invention is directed to methods for reducing blood lactate concentration during exercise, physical activity or athletic performance.
EP1318819A4 Treatment of trauma, and other indications Provided is a method of treating an area affected by a trauma, such as a corneal wound or internal trauma, comprising administering to the affected area a trauma treating effective amount of a composition comprising a polyanionic polymer.
CN102964385A Organic metal ruthenium compound and preparation method and application thereof The invention discloses an organic metal ruthenium compound and a preparation method and application thereof. The chemical name of the organic metal ruthenium compound is 1,7-bi-2-thiophene-1,6-heptadiene-3,5-diketone-methyl isopropylbenzene ruthenium chloride (II). The preparation method comprises the following steps of: 1) dissolving RuCl3.xH2O and gamma-terpinene into ethanol, carrying out heating reflux and stirring for six hours to obtain a product A; 2) dissolving acetylacetone and thiophenecarboxaldehyde into ethanol solution, heating the solution to 80 DEG C, standing for four hours and precipitating out 1,7-bi-2-thiophene-1,6-heptadiene-3,5-diketone; and 3) dissolving the products obtained in the steps 1) and 2) into absolute ethyl alcohol and carrying out heating, stirring and reflux for six hours to obtain the product-1,7-bi-2-thiophene-1,6-heptadiene-3,5-diketone-methyl isopropylbenzene ruthenium chloride (II). The preparation method is simple and low in cost; raw materials are easily available; and the obtained product is used for preparing the drugs for treating cancers and can be prepared into injections, tablets, pills, capsules, suspending agents or emulsion.
EP2266551A1 Compositions and kits comprising a defined boron compound and methods of their preparation A beverage composition comprising: a) a boron compound; and b) at least 10% water, by weight of the composition; wherein the pH of the composition is at least 2 pH units less than the pKa of the boron compound, and wherein the composition is substantially free of boron-carbohydrate complexes.
CA2843401A1 3-hydroxyanthranilic acid (3-haa) therapy for prevention and treatment of hyperlipidemia and its cardiovascular complications The present invention relates to the use of a tryptophan metabolite, 3- hydroxyanthranilic acid (3-HAA)or a functional analogue thereof, for prophylactic and/or therapeutic treatment of mammals, in special humans, against hyperlipidemia and its cardiovascular complications, i.e atheroma formation, myocardial infarction and heart failure, ischemic stroke and transient ischemic attacks, renal impairment, aortic aneurysms and critical limb ischemia caused by atherosclerosis.
EP2291372A2 Intestinal alkaline phosphatase modulators and uses thereof Disclosed are modulators, i.e., activators and inhibitors, of Intestinal Alkaline Phosphatase (IAP). Also disclosed are methods for treating bacterial infections of the intestinal tract and methods for maintaining the health of the intestinal tract using IAP activators. Further disclosed are methods to assist in weight gain of emaciated patients and those having reduced or negligible fat absorption using IAP inhibitors.
EP1332144B1 Indole derivatives as pde5-inhibitors Compounds of the general structural formula and use of the compo unds and salts and solvates thereof, as therapeutic agents.
CA2549008A1 Selective peroxisome proliferator activated receptor modulators The present invention is directed to a novel compound, its composition and use of a compound having a structural formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomers thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
CN103610790A Topical cleaning solution for bone disease and preparation method thereof The invention discloses a topical cleaning solution for a bone disease and a preparation method thereof. The topical cleaning solution for the bone disease is mainly prepared from the following raw materials in parts by weight: 5-30 parts of dried alum, 5-25 parts of smoked plum, 4-25 parts of borneol,10-45 parts of platycodon grandiflorum and 300-700 parts of spring water. The topical cleaning solution for the bone disease disclosed by the invention is high in safety, small in side effect, good in cooperativity, short in treatment cycle, low in recurrence rate, and simple in preparation method as for treatment of the bone disease, and can treat both symptoms and root causes, the total effective rate is 100%, and the total recovery rate is 88%.
WO2011161245A3 Polymorphs of febuxostat The present invention relates to crystalline form I of Febuxostat as well as to pharmaceutical compositions comprising crystalline form I as an active pharmaceutical ingredient. Furthermore the present invention relates to a further polymorphic form of Febuxostat designated as form II and to a novel solvate of Febuxostat. The present invention also relates to methods of making crystalline form I, form II and the novel solvate of Febuxostat.
WO2010032880A3 Kinase inhibitory substances for cancer The present invention provides an agent for the prophylaxis or treatment cancer, which is superior in the safety and the like. An agent for the prophylaxis or treatment cancer, which contains a kinase inhibitory substance showing pseudo-irreversibility, particularly, an agent for the prophylaxis or treatment cancer, which contains a kinase inhibitory substance showing t1/2 relative to kinase (receptor kinase etc.) of not less than 10 minutes.
WO2008070000A2 Treatment of anxiety with eszopiclone The present disclosure provides a unit dosage form with an anxiolytic dosage of zopiclone particularly eszopiclone. Also provided is a method for treatment or prophylaxis of anxiety using a subsedative dosage of zopiclone particularly eszopiclone.
CN1660080A Drop pills of vitamine EC and preparation method A covered dripping pill of VEC for preventing and treating cardiovascular and cerebrovascular diseases, pigmentation, skin rhagades, etc is prepared from VE ane VC. It is composed of a core prepared from VE and matrix and the coated layer prepared from VC and fine powder of auxiliary.
CN101125836B Costene lactone derivative and medical use thereof The invention provides a compound as shown in a structure formula (I). The compound can be used for inhibiting the expression of TNF Alpha, IL-1 Beta and iNOS or the activity of NF- Kappa B, thereby preventing or curing diseases that are related to the high expression of TNF Alpha, IL-1 Beta and iNOS and high activity of NF- Kappa B, such as autoimmune diseases, tumor or arteriosclerosis, etc. The formula (I) is as follows.
CN102451321A Plaster for treating skin trauma The invention discloses a plaster for treating skin trauma. The plaster comprises, by weight, 16-26% of calcined gypsum, 4-9% of yellow lead, 0.7-1% of menthol, 8-13% of Red Halloysite, 2-6% of dragon's blood, 1-4% of borneol, 40-56% of mercurochrome and 8-13% of catechu. The plaster for treating the skin trauma of the invention, which can treat burns, scalds and other skin trauma, has the advantages of short treatment course, good effect, no need of skin grafting, and less scar after curing.
WO2007011290A1 Bronchorelaxing agents based on indol- and isoquinoline derivatives A compound of formula (I) and its acid addition salts, wherein R1-FIj are H, lower (CrC6) alkyl; halogen; NR5R6, wherein R5, R6 are H, lower alkyl, C2-C6 acyl, SO2R7, wherein R7 is lower alkyl, CF3, aryl, substituted aryl; CN; COR8, wherein R8 is H, OH, lower alkyl, lower alkoxy; SO2R9, wherein R9 is OR10, wherein R10 is H, lower alkyl or NRnR12, wherein R11 and R12 is H or lower alkyl; ORi3, wherein R13 is H, lower alkyl, C2-C6 acyl, C1-C8 carboxy, C1-C8 carbamoyl; X is O or S; A is H, lower alkyl; B is C1-C18 alkyl optionally substituted; M is zero or 1; with the proviso that no more than three of R1-R4 are H, for treating and preventing bronchoconstructive pulmonary disease.
CN101041014A Plaster for treating scald and burn for external application The invention provides a film coating agent for treating scalds and burns, wherein the raw material herbs include (by weight ratio) rheum officinale 7-13 parts, calcined gypsum 5-15 parts, bletilla striata 3-10 parts and glycerin 3-6 parts. The invention also discloses the process for preparing the medicinal agent.
WO2010132547A3 Oxaza heterocyclic compounds for phototherapy The invention relates generally to optical agents, including phototherapeutic agents, for biomedical applications, including phototherapy. The invention includes optical agents, and related therapeutic methods, comprising oxaza compounds, including 1,2 oxaza heterocyclic compounds, having a photolabile N-O bond directly or indirectly linked to at least one carbocyclic aromatic and/or heterocyclic aromatic group. In some embodiments, for example, the invention provides oxaza compounds, such as oxazolines and isoxazolidines, for phototherapeutic methods having a photolabile N-O bond that undergoes photoactivated cleavage to produce reactive species, such as radicals, ions, etc., that achieve a desired therapeutic effect, such as selective and/or localized tissue damage and/or cell death.
CN101898980A Application of ultrafine powder and nanocrystallization technology in preparation of calcium hydroxybenzosulfonate as raw material The invention relates to application of an ultrafine powder and nanocrystallization technology in the preparation of calcium hydroxybenzosulfonate as a raw material. A product is prepared through the following steps of: carrying out heating reflux of hydroquinone and concentrated sulfuric acid for about 1 hour under nitrogen protection to form 2,5-dihydroxybenzenesulfonic acid as a solid, adding water into the solid for stirring, dissolving, adding calcium carbonate for neutralization in several times to enable the pH to be 4.6-6.0, placing to generate calcium sulfate precipitates, filtering, washing calcium sulfate with water in three times, merging filtrates, carrying out decompression concentration until the solid is precipitated, adding alcohol for placing, precipitating crystals to obtain a crude product, then adding the crude product into the water, regulating the pH to be 6.0-7.0, placing to enable the calcium sulfate to be completely precipitated, washing the calcium sulfate with the water, merging the filtrates, adding activated carbon for decoloring, filtering, carrying out decompression distillation and concentration, placing to precipitate the crystals, filtering, drying, and then entering a nanocrystallization pulverizer for pulverization to obtain the product. The product is quite easy to absorb and has high bioavailability, the used dosage and the adverse reaction are reduced, the production cost can be lowered, great advantages are brought to patients, and the usage of medicine raw materials supplies a direction for the future development of preparations.
US20120136058 Method For Increasing The Solubility Of Methionine By Mineral Addition And Acid Treatment The present invention relates to a method for enhancing the solubility of methionine. More particularly, the present invention relates to a method for increasing the solubility of methionine, in which mineral and sulfuric acid are added at an appropriate ratio to enhance the methionine solubility, thereby overcoming the problem of low solubility of methionine in water.
CN101843784A Multi-dimensional xanthophyll preparation for powerfully protecting eyesight The invention relates to a multi-dimensional xanthophyll preparation for powerfully protecting eyesight, which is prepared from raw materials consisting of xanthophyll, taurine, selenium, alpha-lipoic acid, L-ascorbic acid, beta-carotene, DHEA, a grape seed extract and pyridoxine hydrochloride and auxiliary materials in a certain proportion. The preparation can be prepared into tablets, capsules, granules, oral liquid, pills and other common formulations. The preparation is mainly used for myopia, amblyopia, hyperopia, presbyopia, cataract, vitreous opacity, retinitis pigmentosa, macular degeneration, asthenopia, diabetic retinopathy and the like. The preparation adopts a multi-component, multi-path and multi-mechanism unique formula and has obvious treatment effect and positive popularization value.
CN103272053A Topical ointment for treating bedsores and preparation method thereof The invention relates to a topical ointment for treating bedsores and a preparation method thereof. The topical ointment is characterized in that the topical ointment is made from the following raw medicines, by weight, 22-28 parts of codonopsis pilosula, 22-28 parts of lumbricus, 18-22 parts of gallnut, 18-22 parts of rheum officinale, 10-14 parts of poria cocos, 10-14 parts of Chinese angelica, 10-14 parts of frankincense, 9-11 parts of angelica dahurica, 9-11 parts of myrrh, 9-11 parts of radix rehmanniae, 9-11 parts of oldenlandia diffusa, 9-11 parts of lithospermum, 6-8 parts of bighead atractylodes rhizome, 6-8 parts of white peony root, 6-8 parts of coptis, 4-6 parts of licorice, 1-3 parts of borneol, 0.8-1.2 parts of verdigris, and 0.8-1.2 parts of calomel. The topical ointment is advantaged by rapid effects and significant effects without leaving scars. Through clinical verifications, the effective rate of the topical ointment for treating bedsores is 100%. [0]
CN103202854A Povidone iodine compound disinfectant The invention discloses a povidone iodine compound disinfectant. The compound disinfectant comprises the following components in percentage by weight: 5 to 20 percent of povidone iodine, 1 to 5 percent of disodium hydrogen phosphate, 1 to 10 percent of medical glycerol, 0.5 to 2 percent of hydroxyethyl cellulose, 0.1 to 2 percent of nonyl phenol polyether-10, 0.1 to 5 percent of dimethyl silicone oil and the balance of injection water. The compound disinfectant can be used for producing various povidone iodine compound scrubbing sheets, povidone iodine compound cotton swabs, povidone iodine compound sponge mats, povidone iodine compound hand-washing brushes and the like with different sizes, and the products are specially treated or disinfected, so sterility and safety of the products are fully ensured, users can directly use the products after unpacking, and cross contamination and infection of intermediate links are avoided. The compound disinfectant is low in irritation to skin, low in toxicity, lasting in action and safe and convenient to use, substantially does not have irritation to tissues, and is used for disinfection of the skin and mucosa such as pre-operation cleaning, disinfection of operative sites and wounds and cleaning and disinfection of the skin before and after arterial blood drawing.
US6956043 Pharmaceutical compositions comprising 33-epi-chloro-33-desoxy-ascomycin solid dispersions A pharmaceutical composition in the form of a solid dispersion comprising a macrolide, e.g. a rapamycin or an ascomycin, and a carrier medium.
CN1602868A Dripping pills of ketotifen fumarate and its preparation method The invention ketotifen fumarate pill, prepared by superfine crushing and pill producing techniques, can achieve the purposes of increasing disintegration and dispersion speeds, and dissolving-out speed and degree, quickly taking effect, improving drug stability, reducing auxiliary use, reducing production cost, being convenient to carry and take. Its compliance is good and it is especially suitable for children, the aged, patients in bed and patients difficult in swallowing to take.
US7090864 Non-invasive gene targeting to ocular cells Liposomes containing therapeutic genes are conjugated to multiple targeting agents to provide transport of the encapsulated gene across the blood-retinal barrier and the plasma membrane of ocular cells. Once across the blood-retinal barrier and ocular cell membrane, the encapsulated gene expresses the encoded therapeutic agent within the ocular cells to provide diagnosis and/or treatment of disease.
CN101332172A Dipivefrin hydrochlorideusp in-situ-forming eye gel The present invention discloses a dipivefrine hydrochloride in situ forming eye gel and a preparation method thereof. 1000ml of the dipivefrine hydrochloride in situ forming eye gel of the present invention contains 0.1 to 2.5g of dipivefrine hydrochloride, 0.05 to 1g of preservative, 1.0 to 7.5g of osmotic pressure regulator and 30 to 150g of gel substrate, and the rest is acid-base buffer and water for injection. The dipivefrine hydrochloride in situ forming eye gel adopts the optimization of accessories and the technical improvement to enrich the medicine preparation form of the dipivefrine hydrochloride, prolong the resorting time of medicine in eye and improve the curative effect, and the dipivefrine hydrochloride in situ forming eye gel does not cause any bad stimulation effect.
US20120087955 Nanoparticulate megestrol formulations The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.
WO2011000946A1 Gymnemic acids for antifungal applications Described herein are compounds and compositions useful as antifungals and methods of preventing and/or treating mycosis infections is a subject. Some embodiments comprise contacting a fungus with a compound extracted or purified from the plant Gymnema sylvestre. In preferred embodiments, the compound is a gymnemic acid.
WO2007034279A3 C3a antagonists and pharmaceutical compositions thereof Aryl substituted pyrazole compounds according to the formula (I) or pharmaceutically acceptable salts thereof, are provided. These compounds are useful in pharmaceutical compositions as C3a antagonists for treating a variety of medical conditions associated with the Complement cascade. Methods for treating such conditions are also provided.
US20100069492 Production of ultrapure epa and polar lipids from largely heterotrophic culture Eicosapentaenoic acid (EPA) compositions and EPA-rich polar lipids for prophylactic or therapeutic applications are described. Production from certain cultured micro-organisms (like Nitzschia laevis) promotes synthesis of EPA, including polar lipids including EPA. The EPA-rich polar lipids themselves may be used as polar compounds. EPA can be selectively hydrolysed from particular positions in isolated polar lipids by lipase activity, then optionally further purified. The process bypasses reliance on diminishing fish stocks and on physico-chemical processes that may not adequately separate desirable n-3 HUFAs from unwanted products like DHA also found in fish oil and cultured organisms.
EP1684766B1 USE OF 3-AZA-1-OXA-DIBENZO i e,h /i AZULENES FOR THE MANUFACTURE OF PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT AND PREVENTION OF CENTRAL NERVOUS SYSTEM DISEAS AND DISORDERS The present invention relates to the use of compounds from the group of 3-aza-l-oxadibenzo[e,h]azulenes and of their pharmacologically acceptable salts and solvates for the manufacture of a pharmaceutical formulation for the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other neurotransmitters.
WO2005063705A1 Benzene compounds disubstituted with cyclic groups at the 1- and 2-positions Compounds represented by the general formula (1) or (100) have excellent inhibitory activities against cell adhesion and cell infiltration and are useful as therapeutic or preventive agents for various inflammatory and autoimmune diseases caused by the adhesion and infiltration of white blood cells, for example, inflammatory diseases of intestine (particularly ulcerative colitis or Crohn’s disease), irritable bowel syndrome, rheumatic arthritis, psoriasis, multiple sclerosis, asthma, and atopic dermatitis: (1) (100) wherein R10 is optionally substituted cycloalkyl or the like; R20, R21, R22 and R23 are each hydrogen, alkyl, alkoxy, or the like; R30, R31 and R32 are each hydrogen, alkyl, oxo, or the like; and R40 is optionally substituted alkyl or the like.
US20080187589 Multi-modal delivery via transmucosal and gastro-intestinal absorption of antihistamines and symptom relief A multi-modal absorption, medicine-delivery lozenge is provided. The lozenge includes a lozenge base for oral administration into a user's mouth, a medicinal active ingredient including an antihistamine convertible between ionized and non-ionized states, and a buffer present in an effective amount for establishing a pH in the individual's mouth which is characterized by a simultaneous presence of a first pharmacologically effective dose of the non-ionized form of the medicinal active ingredient for transmucosal absorption, and a second pharmacologically effective dose of the ionized form of the medicinal active ingredient for gastro-intestinal absorption.
WO2013160645A1 Dexanabinol or a derivative thereof for use in the treatment of cancer in dose ranges of 2-30 mg/kg There is described a method of treating cancer in a patient wherein the method comprises the administration of dexanabinol, or a derivative thereof, in an amount of from about 2mg/kg to about 30mg/kg, based op the weight of the patient.
EP1263444B1 Use of xanthine derivatives for preparing a medicine for preventing and treating osteoporosis . The invention concerns the use of a xanthine derivative of formula (I) and its physiologically acceptable salts for preparing a medicine for preventing or treating osteoporosis, wherein: R1, R2 and R3 are as defined in the description.
CN103599071A Preparation method of polyinosinic-polycytidylic acid dry powder The invention provides a preparation method of polyinosinic-polycytidylic acid dry powder. The method comprises the following steps: (1) respectively dissolving polyinosinic acid and polycytidysic acid in a phosphate buffer solution, mixing the solution, adding a stabilizer, uniformly mixing the stabilizer and the solution, and performing heat preservation on the mixture at the temperature of 40-100DEG C; (2) naturally cooling the reaction liquid obtained in the step (1), mixing the reaction liquid with an organic solvent, standing for precipitating, and drying the precipitate, thereby obtaining the polyinosinic-polycytidylic acid dry powder. The preparation method has the beneficial effects that the prepared polyinosinic-polycytidylic acid dry powder has a complete double-helix structural features and physiological activity, the quality and the stability are better than those of the polyinosinic-polycytidylic acid at a solution state, a stronger enzymolysis-resisting performance can be achieved compared with the bare polyinosinic-polycytidylic acid after entering a living body, so that the curative effect can be enhanced. The polyinosinic-polycytidylic acid is purified in the process for making the polyinosinic-polycytidylic acid solution into the dry powder, a plurality of small-molecular-weight substances and impurities can be removed, the toxic and side effects can be reduced, and the quality of the polyinosinic-polycytidylic acid can be improved.
CA2500712C Antibiotic pharmaceutical composition with improved oral absorbability An objective of the present invention is to provide a cefditoren pivoxil pharmaceutical preparation which can safely be administered to a patient and not only improves wettability of cefditoren pivoxil, but also further improves absorbability through the intestinal tracts by maintaining amorphous particles having a high oral absorbability in a liquid for a long period of time. The present invention is a pharmaceutical composition comprising amorphous cefditoren pivoxil and a sucrose ester fatty acid, which is obtainable by mixing or wet-granulating particles containing amorphous cefditoren pivoxil with the sucrose ester fatty acid while amorphous cefditoren pivoxil maintains its particle state.
US20120245230 Method and composition for preparing stable liquid formulations of paracetamol The present invention relates to stable liquid formulations of paracetamol for pharmaceutical use and to a method of preparation of stable paracetamol solutions.
CN103044514A Preparation method of 3beta-hydroxy-6-thiosemicarbazone steroid metal complex and application of metal complex in antineoplastic drug The invention discloses a 3beta-hydroxy-6-thiosemicarbazone steroid metal complex having a different branched chain structure. A chemical structural formula of the metal complex is as Formula I as shown in the specification, wherein M in Formula I is Pt (II) and Cu (II). The 3-hydroxy-6-thiosemicarbazone steroid metal complex with the different branched chain structure is obtained by starting from cholesterol, sitosterol or stigmasterol, performing pyridinium chlorochromate oxidization, and sodium borohydride selective reduction, then performing 6-carbonyl functional group transformation, and further performing metal ion coordination. An experiment proves that the 3-hydroxy-6-thiosemicarbazone steroid metal complex with the different branched chain structure has an obvious inhibition effect on various tumor cell strains, and can be applied in preparing a drug for treating a cancer.
US20100098733 Nitric oxide releasing particles for oral care applications The present invention provides an oral care composition Comprising a nitric oxide releasing particle and an orally-acceptable carrier. The nitric oxide releasing particle comprises at least one nitric oxide donor. Another aspect of the present invention provides a device for oral care comprising a nitric oxide releasing particle, wherein the device is configured to expose a targeted site in an oral cavity of a subject to nitric oxide. The present invention also provides methods and uses of providing oral health benefits by using the oral care compositions or devices as described above.
CN102391180A Sulfydryl-containing tacrine derivative and preparation method and application thereof The invention provides a sulfydryl-containing tacrine compound or a dynamic isomer or a medicinal salt thereof. The compound or the dynamic isomer or the medicinal salt thereof have the functions of suppressing acetylcholine esterase, enhancing sea horse LTP (Long-Term Potentiation) and improving learning and memory, and can be used for treating, improving or preventing cognitive function decline-related neurous system diseases such as the Alzheimer's disease, vascular dementia, mild cognitive impairment and other oxidative stress participated dementia.
US20120082634 Treatment for dyslipidemia The present invention relates to compounds, and compositions, useful for treating dyslipidemia.
CN1927223A Fat-reducing and beauty nourishing capsule The invention relates to a capsule made from fat metabolism adjusting peptide, tea peptide, conjugate linolic acid, L- carnitine, carnitine, mannan, veralkamine, iron, chromium, and vitamin. The inventive production comprises weighting, mixing, stuffing capsule, sealing, checking and packing. The invention can be used to slim, reduce blood pressure, and restrain cancer, etc.
CN1761457B Amoxicillin trihydrate The present invention relates to a product of amoxicillin trihydrate, having a free water content of less than 0.1 wt.%, preferably less than 0.07 wt.%, more preferably less than 0.05 wt.%, measured at an equilibrium relative humidity of 30% and at a temperature of 25 DEG C. The product is advantageously used in mixture with clavulanic acid. The invention also relates to a process for the preparation of the new product.
US20120328519 Dentric polyglycerol sulfates and sulfonates and their use for inflammatory diseases The present invention relates to the novel compound classes of dendritic polyglycerol sulfates and sultanates as well as to their production and use for the treatment of diseases, particularly inflammatory diseases, and to their use as selectin inhibitors and selectin indicators. The dendritic polyglycerol sulfates and sulfonates are also suitable for imaging diagnostics, particularly with respect to inflammatory diseases.
CN1568997A Antibacterial cooperated pharmaceutical composition The invention relates to a composition of antibiotic synergistic agent and antibacterial drug, wherein the composition comprises Trimethoprin (TMP) or its medicinal salts and Levofloxacin antibacterial medicament and their medicinal salt mixture, the composition also contains bulking agent, thinning agent and allocating material.
CN101264214A Medicaments for treating cervical erosion and preparation thereof The invention relates to a medicine for curing cervix erosion, comprising the following components and contents (weight percentage): lime 38 percent to 42 percent, poria cocos 10 percent to 15 percent, radix onosmatis 10 percent to 15 percent, buckwheat ash 10 percent to 15 percent, honeysuckle stem 10 percent to 15 percent and borneol 3 percent to 5 percent. The preparation method of the medicine comprises the following steps: step 1: taking radix onosmatis 100 grams and buckwheat ash 100 grams, adding purified water 300 ml, and immersion for three to five days under the normal temperature, then taking the supernatant 200 ml with a filter; step 2: taking honeysuckle stem 100 grams, poria cocos 100 grams, borneol 35 grams and lime 300 grams, adding an amount of water, boiling for one hour under a high temperature to concentrate to about 600 ml, after cooling, taking the supernatant 500 ml; step 3: mixing the 200 ml supernatant and the 500 ml supernatant together to acquire 700 ml fluid, then mixing uniformly, and natural sedimentation for one day, then taking the supernatant 500 ml, and packing with a ceramic bottle for sealing, so that the medicine for curing cervix erosion is acquired. The invention has the advantages of completely curing cervix erosion, simple and easy practice, no high-low temperature, and no poison and side effect to human body.
WO2014014270A1 Isoquinoline-5-carboxamide derivative having inhibitory activity for protein kinase Isoquinoline-5-carboxamide derivative, expressed by chemical formula 1, and pharmaceutically acceptable salts, isomers, hydrates, and compounds selected from solvates thereof are useful in preventing or treating diseases with abnormal cell growth.
WO2006004458A1 Biologically active astaxanthin-containing agent The invention relates to biologically active preparations and is used for producing bioactive astaxanthin-containing agents exhibiting a high antioxidant activity. The aim of said invention is to rationally optimise a component composition of biologically active preparations, thereby attaining a technical results of increasing the agent biological activity, in particular the antioxidant activity thereof. Said aim is attained by the use of a biologically active astaxanthin-containing agent which is embodied in the form of a liquid or solid mixture of components dissolved therein and comprises an astaxanthin-containing complex of beta-carotene, cantaxanthin, astatine, half-astatine, lutein, zeaxanthin, solvents, auxiliary components and inert fillers. Said invention also relates to an inequality system which interrelates the basic elements of the biologically active agent and is formed in such a way that in order to optimise the composition thereof, the content of each new component in the agent is selected taking into consideration and according to a factual or predetermined content (C) of the entire astaxanthin-containing complex and also to a value C2 which represents a trans-astaxanthin content therein.
US20110008311 Animal Model and Use of 17Beta-Hydroxysteroid Dehydrogenase Type 7 in the Diagnosis of Anencephaly The present invention features a non-human animal in which is deficient in the expression of endogenous 17β Hydroxysteroid Dehydrogenases Type 7 and use of the same in screening methods for agents that prevent or treat anencephaly. The present invention also provides a method for diagnosing and treating.
CN1875982A A composite preparation for treating HP (helicobacter pylori) The invention discloses a composite preparation of Omepraxole and Clarithromycin, wherein the weight ratio of the active constituents Omepraxole and Clarithromycin is 1:10-1:50, the preparation can be used for treating diseases such as Helicobacter Pylori infection.
CN103251593A Repaglinide/metformin composition The invention relates to a repaglinide/metformin composition, particularly a pharmaceutical composition which comprises the following components in parts by weight: 500 parts of metformin hydrochloride, 0.5-5 parts of repaglinide and 10-200 parts of medicinal auxiliary materials. The medicinal auxiliary materials include, but are not limited to filler, disintegrant, binding agent, alkali and lubricant. The invention also relates to a method for preparing the pharmaceutical composition. The pharmaceutical composition provided by the invention has favorable pharmaceutical properties.
US20050153928 Conjugates comprising a central nervous system-active drug linked to glucuronic acid or glucosamine through an amide bond and uses thereof Disclosed are conjugates comprising a central nervous system-active drug linked through an amide bond to a glucuronic acid or glucosamine moiety, and uses thereof, e.g., for treating or ameliorating central nervous system diseases or disorders.
US20120219640 Anti-infective solution for athlete's foot Disclosed herein is a novel use of highly diluted iodine solution in alcohol to effectively treat and prevent athlete's foot skin disease and disinfect and deodorize shoes without staining skin, clothing or surrounding materials.
US20110053948 Pyrrolidines as nk3 receptor antagonists The present invention relates to a compounds of formula I wherein R1, R2, Ar1, Ar2, R′, R″, m, n, and o are defined in the specification or to a pharmaceutically active salt, racemic mixture, enantiomer, optical isomer or to tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
CA2601705A1 Use of wnv dna vaccine in combination with a conventional vaccine to overcome immunogen interference A method, composition and kit for reducing or preventing immunogenic interference in a multi-valent vaccine utilizes a nucleic acid or DNA component along with other non-nucleic acid immunogenic components.
WO2011023392A1 Pharmaceutical combination comprising 6-dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol or 6-dimethylaminomethyl-1-(3-hydroxy-phenyl)-cyclohexane-1,3-diol and an antiepileptic The present invention relates to a combination comprising (a) at least one 6- Dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol component and/or at least one 6-Dimethylaminomethyl-1-(3-hydroxy-phenyl)-cyclohexane-1,3-diol component, and (b) at least one antiepileptic; a pharmaceutical composition comprising said combination, a medicament comprising said combination, a kit as well as a method of treating pain characterized in that components (a) and (b) are administered simultaneously or sequentially, wherein component (a) may be administered before or after component (b) and wherein components (a) or (b) are administered either via the same or a different pathway of administration.
EP2370425A2 Fused imidazole derivatives as trpv3 antagonist The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRP V3. (Formula I) (I)
CN102921009A Novel niacin compound sustained release preparation for treating hyperlipidemia The invention provides a novel niacin compound sustained release preparation for treating hyperlipidemia, which comprises a quick release part and a sustained release part, wherein the quick release part comprises statins and pharmaceutic adjuvants, the sustained release part comprises niacin and pharmaceutic adjuvants, the weight ratio of statins to niacin in the compound preparation is 1: (10-100), and the weight ratio of polyvinylpyrrolidone k90 to niacin in the sustained release part is 1: (20-80). The compound preparation provided by the invention is suitable for treating hyperlipidemia of Asians, and compared with the prior niacin statins sustained release preparation, the compound preparation provided by the invention contains less statins, meanwhile also achieves good curative effect, and the toxic and side effects of the compound preparation are greatly reduced.
WO2013081016A1 Purinone derivative hydrochloride A hydrochloride of 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4- phenoxyphenyl)-7,9-dihydro-8H-purin-8-one, which is a purinone derivative, is a compound having a Btk-selective inhibitory activity and excellent metabolism stability, capable of solubilizing and absorbing a free base satisfactorily, and capable of being crystallized. Therefore, the compound can be used as a therapeutic agent for diseases associated with a B cell or a mast cell.
US20110003768 Prebiotic compositions The present invention concerns nutritional compositions comprising oligosaccharides for controlling inflammatory bowel disease and related disorders, such as diarrhoea and constipation.
WO2013136061A1 New polymorphic form of a long-acting beta-2 adrenoceptor agonist New polymorphic form of a long-acting beta-2 adrenoceptor agonist A new polymorphic form of arformoterol tartrate, designated as form D, is provided and which is characterised by at least one of the following: (i) a powder X-ray diffraction pattern having peaks at approximately 6.8, 13.3, 13.6, 3.8, 14.1, 18.2, 18.7, 20.0 ±0.2 degrees two theta; or (ii) a DSC thermogram showing an endothermic peak with an onset at approximately 19-120 ºC, and a maximum at approximately 129-131 ºC, followed by an exothermic peak with a maximum at approximately 137-138 ºC; wherein the DSC thermogram of form D has a further endothermic peak with an onset at approximately 168-170 ºC.1 Processes for preparing the new polymorphic form, uses thereof and intermediates for the preparation thereof, are also provided.
US20110052524 vertebroplasty method using an addition curable polysiloxane system The invention relates generally to treatments of disordered bony structures, in particular to vertebroplasty compositions and methods and, more specifically, to treating vertebral bodies in living creatures, in particular, human beings and also compositions suitable for use in such methods and preparation and use of such compositions. According to the invention the composition to be used is an addition curable polysiloxane system.
WO2008003667A3 Combinations of monoamine reuptake inhibitors and potassium channel activators This invention provides pharmaceutical compositions comprising therapeutically effective amounts of a monoamine reuptake inhibitor and an SK inhibitor. In another aspect the invention provides novel benzoimidazole derivatives for use according to the invention.
US20100178316 Extended release of bioactive molecules from silicone hydrogels A dosage form for the administration of a biologically active agent is a silicone hydrogel appliance where the agent is absorbed in a copolymer of at least one siloxane containing monomer and at least one hydrophilic monomer where the appliance is placed in contact with a tissue surface of the patient, such as a contact lens placed in the eye. The appliance can be formed where a copolymer of the siloxane containing and hydrophobic monomers is soaked in a solution of the biologically active agent. The agent can be a non-ionic drug which is absorbed into the appliance from a non-aqueous solution, such as an ethanol solution.
CN101919809A New dexpanthenol injection preparation and preparation method thereof The invention discloses a new dexpanthenol injection preparation and a preparation method thereof. The injection is prepared by dissolving an active component of dexpanthenol with injection water, conditioning by a proper pH conditioning agent and sterilizing at high temperature. The invention has the characteristics of reasonable prescription, simple process, easy industrialization, and the like. The injection used as a preventing agent is immediately used after larger abdominal surgery for reducing the possibility of generating paralytic bowel infarction. The new dexpanthenol injection preparation can be applied to abdominal distension caused by anenteroneuria, postoperative or postpartum flatus retention or postoperative delay of bowel motile restoration and paralytic bowel infarction.
WO2009134666A1 Indazole compounds as ccr1 receptor antagonists Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
US20110189300 siRNA SILENCING OF APOLIPOPROTEIN B The present invention provides nucleic acid-lipid particles comprising siRNA molecules that silence ApoB expression and methods of using such nucleic acid-lipid particles to silence ApoB expression.
US8133877 Composition comprising an antisense sequence implicated in the regulation of angiogenesis Therapeutic compositions used in the field of angiogenesis include nucleotide sequences of genes, the involvement of the genes in the angiogenesis mechanism having been demonstrated by the Applicant, and including the complementary sequences thereof, the antisense sequences of same, polypeptide sequences coded by the coding parts of the aforementioned genes and antibodies that are directed against the polypeptide sequences and also relate to genetically-modified cells that underexpress or overexpress the above-mentioned genes and to therapeutic compositions containing the cells, which are used to treat angiogenic disorders, and, moreover, relate to methods of diagnosing and/or prognosticating antigenic disorders and to novel methods of screening active compounds in the treatment of the disorders.
CN101697960A Huperzine-A solid dispersion and method for preparing tablet thereof The invention discloses a huperzine-A solid dispersion and a method for preparing a tablet thereof. The huperzine-A solid dispersion comprises huperzine-A and a carrier used as a dispersant; the weight ratio range of the carrier to the huperzine-A is 1-25:1; the carrier material may be one or more of polyvinylpyrrolidone, polyethylene glycol 4000, polyethylene glycol 6000, Poloxamer 188, mannitol, lactose or microcrystalline cellulose; and the huperzine-A solid dispersion is prepared by adopting a grinding method, and the obtained solid dispersion can be prepared into huperzine-A tablets by adopting a wet granulating and tabletting method. The huperzine-A solid dispersion can remarkably increase the solubility of a medicament and promote the absorption so as to greatly improve the dissolution and bioavailability of the medicament.
US20050095285 Pharmaceutical composition and a process for its preparation The present invention relates to an improved pharmaceutical composition, in the form of a soft gel capsule resistant to digestive juice. The composition of the present invention is made up of gelatin and an enteric polymer in the form of free acid or its salt, containing a benzimidazole derivative used in the treatment of duodenal ulcers, solublised and/or suspended in a liquid or semisolid medium, comprising of a hydrophobic carrier, an alkaline inert to reacting material and a surface active agent and/or a solublising agent. The present invention also relates to a method for preparing the above said pharmaceutical composition.
US20100015152 Diagnostic and therapeutic methods The present invention provides the use of a protein found in breast, prostate, pancreatic and colon cancer cell membranes, known as BCMP 7, in the diagnosis, screening, treatment and prophylaxis of breast, prostate, pancreatic and/or colon cancer, as well as compositions comprising BCMP 7, including vaccines and antibodies that are immunospecific for BCMP 7.
US20110245150 Targets for treatment of chlamydial infections The present invention relates to a screening method for identification of a compound suitable for the prevention, treatment or/and diagnosis of an infection with Chlamydiaceae.
CN102020541A Protein tyrosine phosphatase 1B (PTP1B) inhibitor as well as chemical synthesis method and application thereof The invention relates to a chemical total synthesis method for a new protein tyrosine phosphatase 1B (PTP1B) inhibitor, and application of the PTP1B inhibitor in preparing medicaments for treating type-2 diabetes. The chemical structural formula of the PTP1B inhibitor is shown in the specification, wherein the groups connected with 2, 2', 3, 3' and 6-position carbons of a benzene ring are bromine atoms, and the 4, 4' and 5, 5'-position carbons of the benzene ring are connected with methoxy groups; the chemical name of the PTP1B inhibitor is as follows: (2',3'-dibromo-4',5'-dimethoxy-phenyl)-(2,3,6-tribromo-4,5-dimethoxy-phenyl)-methane. The compound can enhance the sensitivity of an insulin receptor through inhibiting the activity of a protein tyrosine phosphatase-1B, and has a good curative effect on IR (insulin resistance) type-2 diabetes.
US20100160221 Effect of tula on hiv A method of inhibiting a retrovirus production, the method includes administering a retrovirus inhibitor selected from at least one of a TULA protein, a fragment of TULA containing a UBA domain, a UBA domain of TULA, a peptide mimicking TULA, a peptide mimicking a fragment of TULA containing a UBA domain, a peptide mimicking a UBA domain of TULA, a polynucleotide encoding TULA, a polynucleotide encoding a fragment of TULA containing a UBA domain, a polynucleotide encoding a UBA domain of TULA, a polynucleotide encoding a peptide mimicking TULA, a polynucleotide encoding a peptide mimicking a fragment of TULA containing a UBA domain, a polynucleotide encoding a peptide mimicking the UBA domain of TULA, fragments thereof, muteins thereof, variants and splice variants thereof, and combinations thereof to a cell or a tissue infected by a retrovirus.
US20060189578 Method for the synthesis of compounds of formula I and their uses thereof This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
CA2699630A1 Transdermal, alcohol-free, pharmaceutical compositions An alcohol-free, transdermal drug delivery composition administered via a metered spray drug delivery device is described herein. The non-occlusive transdermal drug delivery composition includes a therapeutically effective amount of at least one physiologically active agent or prodrug thereof, an effective amount of at least one dermal penetration enhancer; and at least one non-volatile liquid. The transdermal drug delivery composition is administered to a dermal or mucosal surface of an animal needing the same using a metered spray device capable of delivering a fine spray of substantially uniform particle size to minimize the required drying time therefor.
US20120142631 Medicinal antidiaper rash cream incorporating a biopolymer and a process to make it The present invention is directed to a composition for treating diaper rashes, along with skin rejuvenation containing a) a biopolymer in the form of Chitosan, b) a combination of active pharmaceutical ingredients (APIs), Benzalkonium Chloride & Cetrimide used in treating diaper rashes, c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants, and d) water. The active ingredients, namely chitosan, Benzalkonium Chloride & Cetrimide are incorporated in cream base for use in treating diaper rashes due to allergy & itching, & wounds on human skin involving contacting human skin with the above identified composition.
CN103120666A Application of Aphanamixoid A in medicine for treating human cervical carcinoma The invention discloses an application of Aphanamixoid A in preparation a medicine for treating human cervical carcinoma, and belongs to the technical field of new application of the medicine. The Aphanamixoid A has outstanding inhibiting effect on the growth of human cervical carcinoma cell strains HeLa, HeLa229, HCE1 and CaSKi through in-vitro MTT (Methyl Thiazolyl Tetrazolium) antineoplastic activity evaluation. Thus, the Aphanamixoid A can be used for preparing the medicine for resisting the cervical carcinoma and has good development and application prospect; and the application of the Aphanamixoid A in preparation of the medicine for treating the cervical carcinoma is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on human cervical carcinoma cells is inconceivably high.
WO2014144772A1 Methods of promoting wound healing using crm1 inhibitors The invention generally relates to the use of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I) or a pharmaceutically acceptable salt thereof, wherein Ring A, X, R1, R2 and n are as defined and described herein, in a method for promoting wound healing in a subject.
WO2014079787A1 Substituted 1,6-naphthyridines The present invention relates to the use of compounds of general formula (I) wherein R' is hydrogen or lower alkyl; R1 is halogen, lower alkyl, cycloalkyl or cyano; or is phenyl, optionally substituted by one to three substituents, selected from lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, halogen, cyano, hydroxy, C(O)-NH-lower alkyl, CH2-C(O)-NH-lower alkyl, CH2-NH-C(O)-lower alkyl, CH2NH2, S(O)2CH3, S(O)2N(CH3)2, or by heterocycloalkyl groups; or is pyrazol-1, 4 or 5-yl, optionally substituted by lower alkyl; or is thiazol-5-yl, optionally substituted by one or two lower alkyl groups; or is pyridine 2, 3 or 4-yl, optionally substituted by lower alkyl, lower alkoxy, halogen or N(CH3)2; or is 3,6-dihydro-2H-pyran; or is benzo[d][1,3]dioxol-5-yl; or is 2,3-dihydrobenzo[b][1,4]dioxin-6-yl; R2 is hydrogen, lower alkyl or lower alkyl substituted by alkoxy; R3 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, NH-S(O)2-CH3, -(CH2)m-O-lower alkyl or -(CH2)n-S(O)2-CH3; or is -(CR2)n-phenyl, optionally substituted by -S(O)2CH3 or lower alkoxy; or is -(CH2)n-heterocycloalkyl, optionally substituted by lower alkyl and =O; or is -(CH2)n-heteroaryl, optionally substituted by one or two lower alkyl groups; or is -(CH2)n-cycloalkyl, optionally substituted by cyano; or R2 and R3 form together with the N atom to which they are attached a heterocyclic ring, selected from morpholine, piperidine, 1, 1-dioxo-thiomorpholine or piperazine which may be substituted by lower alkyl or C(O)O-lower alkyl, or may form a pyrrolidine ring, optionally substituted by hydroxy; R is independently from n hydrogen or lower alkyl; n is 0, 1, 2, 3; m is 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, for the treatment of schizophrenia, obsessive-compulsive personality disorder, depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction ("chemobrain"), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs selected from alcohol, opiates, methamphetamine, phencyclidine or cocaine.
CA2789144A1 Compositions and methods for treating obesity and obesity-related conditions A method to effectively treat the adverse events of ingested lipase inhibitor such as orlistat, and to maintain the effectiveness of ingested orlistat, the method comprising the steps of: ingesting a compound of orlistat to irreversibly bind with lipase enzymes of the gastrointestinal tract; ingesting a compound of simethicone to cause undigested fats to remain in an emulsified state in the bowel; and ingesting an enteric-coated activated charcoal to absorb emulsified fats only in the lower bowel, thus preventing the adverse events associated with the ingestion of orlistat alone.
WO2013060274A1 Derivatives of protoberberine biological alkaloids and use of same inhibiting ulcerative colitis Disclosed are derivatives of protoberberine biological alkaloids or physiologically acceptable salts thereof produced by means of a derivative reaction of a source material of biological alkaline quaternary ammonium salts of protoberberine alkaloids, a preparation method for same and pharmaceutical uses thereof. The derivatives of protoberberine biological alkaloids or the physiologically acceptable salts thereof show activity inhibiting ulcerative colitis and can be used in the preparation of drugs for same.
WO2007130616A3 Polyamides for treating human papilloma virus The present invention relates to polyamide compositions and therapies for treating cells infected with human papilloma virus (HPV).
US20060004104 Use of 5-alkyl substituted 2-arylaminophenylacetic acid derivatives as selective cyclooxygenase-2 inhibitors in the treatment of cancer pain, especially bone cancer pain; for example, 5-methyl-2-(2'-chloro-6'-fluoroanilino)-phenylacetic acid The invention provides a method of treating cancer pain, e.g. bone cancer pain, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor; advantageously a compound of formula (I); wherein R, R1, R2, R3, R4, and R5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug ester thereof.
US20120178793 Nucleotide-cochleate compositions and methods of use The present invention is directed to cochleate composition that include a nucleotide. The nucleotide may generally be bound via a linker to a component of the cochleate, or to a lipophilic tail. Additionally or alternatively, the nucleotide may he associated with a transfection agent. The present invention also includes methods for making and using, the compositions provided herein.
EP1602367A1 Transdermal delivery system for treatment of cognitive disorders An improved transdermal delivery composition is provided containing a low molecular weight fatty acid, and a long chain fatty acid or a long chain fatty acid lower alkyl ester, wherein the long chain is between about 1 to about 21 carbons long and preferably, contains at least one cis-olefinic bond. Preferred long chain components are oleic acid and ethyl oleate while the preferred low molecular weight fatty acid is propionic acid. The product may be used for treating a cognitive disorder by administering phenserine through a subject's skin.
WO2010146299A1 Azetidine-derived esters, preparation thereof, and therapeutic use thereof as cannabinoid receptor modulators The invention relates to the compounds of formula (I), where: R is a (C1-C6)alkyl or halo(C1-C6)alkyl group; A is a carbon atom optionally substituted by one or more hydrogen atoms or (C1-C6)alkyl groups; R5 is one or two carbon atoms substituted by one or more groups selected from among the hydroxy, (C1-C6)alkoxy, OCOR2, OCOOR6, or NRaRb groups or a heterocyclic group optionally substituted by a halogen atom or a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, or oxo group; R1 is a hydrogen atom or a (C1-C6)alkyl group; R2 is a hydrogen atom or a (C1-C6)alkyl group; each of R3 and R4 is a phenyl group optionally substituted by one or more atoms or groups selected from among a hydrogen atom, a halogen atom, a (C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group, or a cyano group; R6 is a (C1-C6)alkyl group; Ra and Rb are, independently of each other, a hydrogen atom or a (C1-C6)alkyl group; Y is a hydrogen atom, a halogen, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group, a (C1-C6)alkylS(0)p group, or a cyano group; and p is between 0 and 2 in the state of a base or of an acid addition salt. The invention also relates to a method for preparing same to the therapeutic use thereof.
WO2009081611A1 Antibacterial agent and composition for the oral cavity, food and drink containing the same It is intended to provide a novel antibacterial agent for the oral cavity which has a high safety, excellent blending properties and a potent antibacterial activity against bacteria causative of periodontal diseases and bacteria causative of dental caries. An antibacterial agent characterized by comprising α-linolenic acid monoglyceride or linoleic acid monoglyceride as the active ingredient. This antibacterial agent is appropriately usable as a component of a composition for the oral cavity, a food and a drink.
WO2013064579A1 Use of anti-connexin agents for enhancing the therapeutic effect of acetylcholinesterase inhibitors This invention relates to improvements in therapeutic neurological and neuropsychic treatments using acetylcholinesterase inhibitors. More specifically, the invention enables the effects of the reversible acetylcholinesterase inhibitor donepezil to be potentiated by certain molecules, referred to here as connexin-blocking agents. Said connexin-blocking agent is preferably meclofenamic acid.
EP2586776A1 Soft cationic mitochondrial uncouplers The present invention relates to biology and medicine and in particular can be used in medicine for the preparation of a pharmaceutical composition for the specific, self-regulating uncoupling of mitochondria. The invention can be useful in the treatment of diseases and conditions associated with the disruption of cellular metabolism, in the treatment of obesity, including pathological forms thereof, and also for the treatment of diseases associated with the increased formation of free radicals and reactive oxygen species.
EP2016939A1 Transdermally absorbable preparation comprising anti-dementia agent Disclosed is a percutaneous absorption preparation which enables the stable administration of an antidementia drug over a long period of time. More particularly, the percutaneous absorption preparation of the antidementia drug which is used as a plaster on skin comprises at least an adherent layer, an intermediate membrane, and a drug reservoir layer sequentially from the side which is plastered on skin, wherein the drug reservoir layer comprises at least an antidementia drug, an aminated polymer, a polyhydric alcohol, and one or more carboxylic acid esters, the intermediate membrane enables the controlled permeation of the antidementia drug into the side of skin, the adherent layer enables the plastering of the percutaneous absorption preparation on skin, and is permeable to the antidementia drug.
CN101744801A Application of salvianolic acid B in salvia miltiorrhiza The invention discloses application of salvianolic acid B in salvia miltiorrhiza in preparing a medicament for treating erectile dysfunction, wherein the unit dosage of the salvianolic acid B is 10-500mg. Proved by pharmacological experiments and clinical experiments, the invention has the advantages of small side effect, wide therapeutic window, and the like. After the medicament is taken, the medicament cannot generate after effects on patients, and has the characteristics of natural medicaments. The medicament has good pharmacological action.
WO2013179248A1 Pharmaceutical compositions of pemetrexed A pharmaceutical composition of Pemetrexed represented by formula (I), which is a liquid ready to use solution formulation or a lyophilized pharmaceutical composition for parenteral administration comprising a pharmaceutically acceptable organic amine, an inert gas and optionally containing at least one or more pharmaceutically acceptable excipients. Also provided are processes for preparation of the ready to use solution formulation or lyophilized pharmaceutical composition of the present invention.
WO2011141713A1 New bicyclic compounds as pi3-k and mtor inhibitors There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
US20110274682 Methods for protease assisted protein delivery A method for intracellular delivery of single proteins or other cargo molecules by encapsulation within nanocapsules formed by interfacial polymerization of one or more types of monomers and selected protease cleavable cross-linkers is provided. The thin positively charged capsules are readily brought into the cytosol of target cells by endocytosis. The capsules are degraded by the action of endogenous proteases or co-delivered proteases on the cross-linkers releasing the functional cargo unaltered. The cross-linkers can be adapted to be cleavable by specific enzymes selected from available intracellular enzymes within the target cell or co-delivered or self-cleaving when the cargo itself is a protease. The nanocapsules produced by the methods have been shown to have long-term stability, high cell penetration capability, low toxicity and efficient protease-modulated specific degradability without affecting cargo protein function.
US20110020442 Taste Masked Oral Composition of Telithromycin The invention relates to an oral compositions comprising telithromycin that have taste masking properties, a process for the preparation thereof, and methods of using the composition.
WO2012103116A1 Pulmonary administration of rifalazil and analogs thereof Methods for treating bacterial lung infections, such as tuberculosis infections, using a poorly absorbable form of rifalazil, are described. Compositions for pulmonary administration of a non-microgranulated rifalazil formulation are also described. In one embodiment, the patients that are treated are immuno-compromised, for example, by co-infection with HIV, HBV, or HCV. The delivery of rifalazil in a poorly absorbed form reduces potential adverse events that might result from systemic delivery, and the local delivery to the lungs allows targeted treatment. Where the particles are both relatively large and porous, delivery can be to the deep lung, and systemic delivery can be largely avoided.
WO2013039488A1 Formulations of histone deacetylase inhibitor in combination with bendamustine and uses thereof Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include bendamustine, or a pharmaceutically acceptable salt thereof and an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.
WO2011024056A2 An improved process for the preparation of bosentan The present application provides purification of Bosentan crude by making its crystalline potassium salt, which is further converted to Bosentan (I) with bis-sulfonamide (VIII) and deshydroxyethyl (IX) impurities to less than 0.2% by HPLC analysis.
US7476400 Liposomes containing an oil phase comprising topical anestheic, a C14-C20 alcohol, an alkyl ester of a fatty acid, propylene glycol, and a polyoxyalkylene stearate. A composition comprising lidocaine-containing liposomes wherein the weight concentration of lidocaine in said composition is greater than 10%. The composition is prepared by mixing water with an oil phase comprising lidocaine, a C14-C20 alcohol, an alkyl ester of a fatty acid, propylene glycol, and a polyalkyl stearate. The non-aqueous phase may also include a phospholipid such as phosphatidyl choline.
US20130022643 Antimicrobial Anti-chafing Chelated Silver Oxide Compound Described herewithin is a composition comprising an anti-chafing balm with C18-36 acid triglycerides, capric/carprylic triglycerides, and tribehinin together with a chelated silver oxide complex comprising a barrier film when applied to the skin. The film is a dual purpose antibacterial and anti-chafing barrier topically applied to human skin, providing a layer of chelated silver oxide complex further comprised of a dermatologically acceptable carrier, with friction (chafe) reducing properties, selected from the group consisting of organic solutions, gels, liquids, balms, aerosols, emulsifiers, lotions, water-in-oil emulsions, oil-in-water emulsions, surfactants, aloe barbedensis leaf juice and tocopherol acetate.
CN102614205A New application of stilbene glucoside to preparation of skin ageing-resistant medicaments The invention provides new application of stilbene glucoside to the preparation of skin ageing-resistant medicaments. The stilbene glucoside has the effect of clearing oxygen radicals, can also repair cells damaged because of the accumulation of the oxygen radicals in an ageing process, and overcomes the detects that a skin ageing-resistant medicament has one effect and cures the symptoms but not the disease. The stilbene glucoside can be applied to the preparation of the skin ageing-resistant medicaments. The stilbene glucoside and pharmaceutically acceptable salts, esters or sugars and excipients thereof and the like are applied to the preparation of the medicaments for preventing or treating skin ageing state. The stilbene glucoside and the pharmaceutically acceptable salts, esters or sugars and excipients thereof and the like can be prepared into pharmaceutically acceptable orally taken and externally used preparations and formulations, such as tablets, capsules, liniments, medicinal extracts, coating agents, emulsions, nanoparticle emulsions and the like. The stilbene glucoside has wide application prospect in aspects of medical healthcare and the like.
CN1850764A 6,7-dehydroxyleanone in salvia farinacea root with platelet aggregation inhibition This invention relates to distill restraining blood platelet agglomeration from Xinjiang sage preparation method and pharmacodynamics experiment. The result reveals that comparing to normal saline, 6, 7-dehydrogenation enumerates ketone 2mg/ml group blood platelet restrain ratio is 56.2 percent, and 1mg/ml group blood platelet restrain ratio is 49.7 percent. So 6, 7-dehydrogenation enumerate ketone or extract contains it has good application of restrain blood agglomeration function and in anti cardiovascular diseases.
US20050080057 reducing weight in mammals; Substituted with a thio, sulfoxy or sulfonyl group eg 5-Chloro-2-methylsulfonylindan-1-ol, 5-Chloro-2-(propane-2-sulfonyl)indan-1-ol, 5-Chloro-2-ethanesulfonylindan-1-ol Embodiments of the invention relate to methods of reducing weight in mammals and for the prophylaxis or treatment of obesity comprising administration of of C2-substituted indan-1-ol systems and their physiologically acceptable salts and physiologically functional derivatives. Compounds for use in the methods of the embodiments of the invention include compounds of the formula (I) in which the radicals are as defined, and their physiologically acceptable salts.
US20120252791 Heterocyclic GTP Cyclohydrolase 1 Inhibitors For the Treatment of Pain The present invention relates to the field of small molecule heterocyclic inhibitors of GTP cyclohydrolase (GCH-I), or a tautomer, prodrug, or pharmaceutically acceptable salt thereof. The invention also features pharmaceutical compositions of the compounds and the medical use of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, or neuropathic pain).
US20100196426 Use of microvesicles in diagnosis and prognosis of medical diseases and conditions The presently disclosed subject matter is directed to methods of aiding diagnosis, prognosis, monitoring and evaluation of a disease or other medical condition in a subject by detecting a biomarker in microvesicles isolated from a biological sample from the subject.
CA2412164C Amidine derivatives as selective antagonists of nmda receptors A class of styryl amidine derivatives which are antagonists of the hum NMDA receptor, being selective for those containing the NR2B subunit, are active in the treatment and/or prevention of neurological and neurodegenerative disorders, in particular neuropathic pain and headache, specifically migraine, whils displaying fewer ataxic and related side-effects associated with other classes of NMDA receptor antagonists.
US20060014709 Drug or cosmetic The present invention provides pharmaceuticals or cosmetics, which prevent sclerotic lesions causing apoptosis, degeneration, fibrosis and atrophy, and repair and regenerate the lesions selectively, comprising a compound which preferentially increases regeneration-promoting macrophages and a method for screening the compound which preferentially increases regeneration-promoting macrophages. Pharmaceuticals or cosmetics of the present invention are useful for renal lesions, pancreatic lesions and skin lesions, because these induce regeneration-promoting immunocompetent cells lesion-selectively against organ tissue disorders and cause repair and regeneration thereof.
EP1617837A1 Composition for preventing or treating allergic disease using black rice extract and its therapeutic use The present invention relates to a composition for preventing or treating allergic diseases using black rice extract and its therapeutic use. More precisely, the present invention relates to a composition for preventing or treating allergic diseases comprising pelargonidin, cyanidin glycoside, or black rice extract including pelargonidin and cyanidin glycoside, which inhibit eosinophile accumulation in tissues, as an effective ingredient and a therapeutic use thereof. Pelargonidin, cyanidin glycoside or black rice extract including pelargonidin and cyanidin glycoside inhibit the accumulation of eosinophile in tissues and allergic inflammations thereby, so that they can be effectively used for preventing or treating allergic diseases associated with inflammation and eosinophile accumulation, such as allergic rhinitis, allergic conjunctivitis, asthma, chronic obstructive pulmonary disease, atopic dermatitis and allergic diarrhea, etc.
CA2167525C Fungicidal methods and compositions for killing yeast and sporular microorganisms Methods and compositions are provided for killing or inhibiting the growth of yeast or sporular microorganisms, in the presence of a peroxide and chloride or bromide, with a haloperoxidase and at least one antimicrobial activity enhancing agent. Suitable antimicrobial activity enhancing agents include certain alpha-amino acids, and are preferably compounds of formula (I) wherein R1 is hydrogen, and unsubstituted, or hydroxy or amino substituted straight or branched chain aklyl group having 1 to 6 carbon atoms, or an unsubstituted, or hydroxy or amino substituted arylalkyl group having from 7 to 12 carbon atoms, and R2 is hydrogen or straight or branched chain alkyl group having from 1 to 6 carbon atoms.
CN102964401A Method for preparing clindamycin phosphate The invention relates to a method for preparing clindamycin phosphate, belonging to the field of medicine technologies. According to the method, clindamycin phosphate containing dehydro-clindamycin phosphate is taken as a raw material and dissolved into water or water-containing alcoholic liquid, 1/5-1/100 of the raw material amount of palladium carbon is added, hydrogen is introduced to react for 1-48 hours while stirring, the dehydro-clindamycin phosphate is enabled to fully produce the clindamycin phosphate, and then crystallization is carried out. The method has the advantages that the dehydro-clindamycin phosphate can be enabled to fully produce the clindamycin phosphate, so that the content of impurities in drugs is reduced, and the quality of the drugs is improved.
WO2014111465A1 Isomannide derivatives as inhibitors of soluble epoxide hydrolase The present invention relates to compounds of the formula (I), wherein R1, R11, R12 and X have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They are highly potent and selective soluble epoxide hydrolase inhibitors and are suitable, for example, for the therapy and prophylaxis of renal failure, diabetic nephropathy, type 2 diabetes mellitus, inflammation or could show beneficial effects in pain, dyslipidemia and atherosclerosis. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
EP2769738A1 Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists The present invention relates to a conjugated compound of Formula I : Q-Z-R4 wherein Q is a TLR7 and/or TLR8 agonist and Z-R4 is a TLR2 agonist, said conjugated compound being chosen among compounds of Formula II :
CN101062909A HIV-1prolease peptide mimic new inhibitor having biological activity, preparation method and usage The invention discloses a formula (I) compound, which is characterized by the following: setting n as 0, 1, or 2; expressing R1 as phthalimide group, 2-naphthoxy, 3-naphthoxy, phenoxy, 2-metyl group phenoxy, 2-methoxy phenoxy, 3-methoxy phenoxy, 4-methoxy phenoxy, 2, 6-dimethyl phenoxy, 3-nitro group phenoxy, 3-amido phenoxy, 4-nitro group phenoxy, 4-amido phenoxy, 2-nitro group phenoxy, 2-amido phenoxy, indole-3-methylene, tetrazoline group, triazine azoles group, benzosulphimide group and 2-benzoxazoles ketone; expressing R2 as hydrogen atom, C1-C4 alkyl group and -CH2OH; expressing R3 as tert-butyl group, isobutyl group, benzyl group and cyclopropyl metyl group; expressing R4 as -NHCOCH3, methoxy, amido, nitro group, fluorine atom, chlorine atom and bromine atom.
CN103483388A Norharman-ruthenium (II) polypyridine complex with antitumour activity The invention discloses a preparation method for a Norharman-ruthenium (II) polypyridine complex and the antitumour activity thereof. The chemical formula of the Norharman-ruthenium (II) polypyridine complex disclosed by the invention is [Ru(tpy)(Norharman)3]<2+>(tpy=2,2':6',2''- terpyridyl, Norharman=9H-pyridino-[3,4-b] indol), and prepared by taking ruthenium trichloride and Norharman as raw materials, and performing the steps of heating reflux reaction, cooling and filtering, washing, drying and the like. The influence of the complex on tumour cells is researched in in-vitro antitumour activity test, and the complex is found to be strong in an inhibition effect on the growth of tumour cells HeLa, HepG2, A549, MCF-7, NCI-H460, Bel-7402 and HCT-116. The complex is indicated to be good in a tumour inhibition effect by animal test data, and expected to be a novel antitumour medicinal member, and wide in application prospect.
WO2008067639A1 Composition for promoting weight loss comprising yohimbine, evodia rutaecarpia extract and l-carnitine A nutritional composition and method is provided for promoting weight loss or weight maintenance in an individual by supporting and enhancing thermogenesis and lipid oxidation comprising therapeutically effective amounts of yohimbine from the bark of the tree Corynanthe yohimbe, an effective amount of Evodia rutaecarpia extract and a source of an effective amount of L-carnitine The composition further comprising at least one of Yerba mate, black tea, white tea, Theobromo cacao, caffeine and white willow bark.
WO2010069147A1 Dihydropyrimidine derivatives, compositions thereof and their use Dihydropyrimidine derivatives, their isomers, enantiomers, salts and hydrates, process for preparation thereof, and pharmaceutical compositions thereof are provided. The said compounds can be used in manufacture of medicaments for treating and preventing viral diseases preferably hepatitis B infection.
WO2011012896A3 Spirocyclic amide derivatives Spirocyclic amide derivatives of formula (I) wherein ArCH2CH2NH- represents a β-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.
US20090192133 Treatment for achondroplasia The present application provides, inter alia, methods of treating disorders mediated by FGFRs and methods of screening for Hsp90 inhibitor compounds.
EP1633376B1 Compositions for prevention and treatment of cold and influenza-like symptoms comprising chelated zinc The present invention is directed to respiratory tract compositions, particularly nasal compositions, that are highly effective in the prevention and treatment of cold and influenza-like symptoms due to respiratory tract viral infections. These compositions comprise chelated and unchelated zinc ions, wherein the quantity of chelated zinc ions is at least about 50.1%.
CA2356912C Pharmaceutical compositions for the treatment of ocular hypertension or glaucoma By combined administration of a non-FP receptor agonist type prostaglandin compound, for example isopropyl unoprostone, and a FP-receptor type prostaglandin compound, for example Latanoprost, the ocular hypotensive effect of the prostaglandin compounds is synergistically enhanced.
WO2005121160A3 11, 12 cyclic thiocarbamate macrolide antibacterial agents The present invention is directed to novel macrolide antibacterial agents and processes for preparing them. The present invention is further directed to pharmaceutical compositions containing the novel macrolide antibacterial agents disclosed herein and their use in the treatment and prevention of bacterial infections.
WO2014102824A1 Diclofenac composition The present invention relates a composition comprising Diclofenac and salts thereof wherein Diclofenac or its slats are present in an amount of 25 - 200 mg. The composition is suitable for the parenteral administration through intramuscular, intravenous route; also for oral, dermal, subcutaneous, cutaneous, nasal, ocular drops, as rectal suppository, vaginal pessaries, intra-articular, and otic delivery. The invention also provides compositions comprising a combination of Diclofenac and other drugs. The invention further provides a method for preparing said composition.
US20120208814 Thetrahydroquinolines Derivatives As Bromodomain Inhibitors Tetrahydroquinoline compounds of formula (I) or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicted.
WO2005011703A1 2-cyano-1,3,5-triazine-4,6-diamine derivatives The invention relates to the use of a 2-cyano-1,3,5-triazine -4,6-diamine derivative having general formula (I), wherein R1 is (C1-6)alkyl, (C3-8)cycloalkyl, aryl, aryl(C1-4)alkyl, aryloxy(C1-4)alkyl, heteroaryl or heteroaryloxy(C1-4)alkyl; R2 is H or (C1-4)alkyl; or R1 and R2 together with the nitrogen to which they are bound form a 4-8 membered heterocyclic ring, optionally further comprising 1 or more heteroatoms selected from O, S or NR5, which ring may be substituted with (C1-4)alkyl, (C3-8)cycloalkyl, aryl, aryl(C1-4)alkyl or NR6R7,and which ring may be fused to a benzene ring; R3 is (C1-6)alkyl, (C3-8) cycloalkyl (optionally comprising 1 or more heteroatoms selected from O, S or NR8), aryl, aryl(C1-4)alkyl or heteroaryl; R4 is H or (C1-4)alkyl; or R3 and R4 together with the nitrogen to which they are bound form a 4-8 membered heterocyclic ring, optionally further comprising 1 or more heteroatoms selected from O, S or NR9; R5, R8 and R9 are independently H, (C1-4)alkyl, (C3-8) cycloalkyl, aryl or aryl(C1-4)alkyl; R6 and R7 are independently H or (C1-4)alkyl; or R6 and R7 form together with the nitrogen to which they are bound a 4-8 membered heterocyclic ring; or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of osteoporosis and atherosclerosis.
US7541375 Azole derivatives and pharmaceutical compositions containing them The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing various cancers, inflammation, septic shock, preterm labor, infertility, pain, and ischemia, and other diseases and disorders associated with MEK-1 and/or ERK-2 activation.
US20090041856 Methods for promoting hair growth The present invention relates to methods of promoting hair growth in a patient. The method comprises administering to a patient in need thereof a sugar compound that is converted to a glycosaminoglycan in the patient, a primary antioxidant component, at least one amino acid component, and one or more transition metals.
US20110034719 Process for the preparation of (s)- naproxen 4-nitrooxybutyl ester The present invention relates to a new process for the preparation of the (S)-naproxen 4-nitrooxybutyl ester and to new intermediates obtained and used therein. The invention further relates to the use of the new intermediates for the manufacturing of pharmaceutically active compounds such as (S)-naproxen 4-nitrooxybutyl ester. The invention also relates to the use of (S)-naproxen 4-nitrooxybutyl ester prepared according to the process of the present invention for the manufacturing of a medicament for the treatment of pain.
WO2011153493A2 Biodegradable lipids for the delivery of active agents The present invention relates to a cationic lipid having one or more biodegradable groups located in the mid- or distal section of a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.
CN1857288A Slow released compound preparation of glycyrrhizic acid and glycyrrhizinate and its preparing process The present invention discloses a kind of slow released compound preparation of glycyrrhizic acid and its salt. The slow released compound preparation consists of: glycyrrhizic acid or its salt, amino acid and framework material in the weight ratio of 1 to 0.4-11 to 0.1-15. The present invention also discloses the preparation process of the slow released compound preparation. Compared with available tablet of glycyrrhizinate, the slow released compound preparation has the advantages of high bioavailability, less side effect, more indications, etc.
US6946141 As-needed administration of tricyclic and other non-SRI antidepressant drugs to treat premature ejaculation A method is provided for treatment of premature ejaculation by administration of an antidepressant drug selected from tricyclic antidepressants, tetracyclic antidepressants, MAO inhibitors, azaspirone antidepressants, and atypical non-SRI antidepressants. In a preferred embodiment, administration is on as “as-needed” basis, i.e., the drug is administered immediately or at most several hours prior to sexual activity. Pharmaceutical formulations and packaged kits are also provided.
WO2013154707A1 Co-polymer conjugates This application relates generally to biocompatible water-soluble polymers with pendant functional groups and methods for making them, and particularly to co-polymer polyglutamate amino acid conjugates useful for a variety of anti-cancer drug delivery applications.
CN102924302A Injection-grade ambroxol hydrochloride and solution for inhalation of injection-grade ambroxol hydrochloride The invention relates to a method for refining injection-grade ambroxol hydrochloride. The method is characterized by comprising the steps of adding oral-taking-grade ambroxol hydrochloride with the proportion smaller than or equal to 20:1 into ethanol water solution with the volume ratio of 5-20%; performing heating to completely dissolve the oral-taking-grade ambroxol hydrochloride; stopping heating and performing cooling to seed out ambroxol hydrochloride; and filtering solvent to obtain crystals and drying the crystals to obtain the injection-grade ambroxol hydrochloride. The invention further relates to ambroxol hydrochloride solution for inhalation prepared by utilizing the prepared injection-grade ambroxol hydrochloride as the raw material. The atomization inhalation solution comprises the ambroxol hydrochloride, a stabilizer, a pH conditioning agent and an osmotic pressure conditioning agent. By means of the scientific preparation adopting the carrier, fewest degradation products of the atomization inhalation preparation can be produced under the high temperature of 121 DEG C for 15 minutes, the atomization inhalation preparation is stable, and the service life of the atomization inhalation preparation is prolonged to 5 years.
CN101156842A Pharmaceutical preparation containing arginine glutamic acid The invention relates to the medicament preparation of arginine glutamic acid and the preparation method and the application thereof. Through long-term experimental study, the personnel of the invention develops the medicament preparation of the arginine glutamic acid, the preparation takes the arginine glutamic acid as raw material medicine, which prepares the preparation with proper medicinal auxiliary material. The operating process of the medicament preparation of the invention is simple, the environmental pollution is small, and the invention is suitable for the production of a great industry. A pharmacological test shows that the medicament preparation of arginine glutamic acid has a very obvious pharmacological function on the aspect of the remedy of the hyperammonemia caused by acute liver disease and chronic liver disease such as hepatocirrhosis, fatty liver and hepatitis.
WO2009074157A1 Fully-modified phenyl pyrrole aminoguanidines The invention relates to phenyl pyrrole aminoguanidines modified at the guanidine group of the general formula (I), including tautomeric and isomeric forms thereof, wherein, X is (II) and i is 0,1or 2, Y is (III) and j is 0 or 1; wherein Q is nitrogen (N) or carbon (C), and ∪ represents, together with Q and the carbon atom covalently linked to Q, an optionally substituted five-or six-membered heterocyclyl or cycloalkyl group; and Z is (IV) and k is 0,1,2 or 3. The invention further relates to the use of such modified phenyl pyrrole aminoguanidines for the treatment of diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones. Such diseases include inflammatory diseases, metabolic syndrome, insulin-resistance, diabetes mellitus, and obesity.
US20120263698 Treatment of Neurodegenerative Disease A method for reducing alpha-synuclein amyloid protein in a patient suffering from Parkinson's Disease comprising administering to the patient an effective amount of trans-resveratrol, a method for treating a neurodegenerative disease associated with amyloid proteins comprising administering to a patient in need thereof an effective amount of trans-resveratrol, and a method for treating Parkinson's Disease comprising administering to a patient in need thereof a pharmaceutically effective amount of carbidopa, levodopa, and trans-resveratrol are described. More particularly, the effect of trans-resveratrol on reducing the pharmaceutically effective dose of at least one of carbidopa and levodopa in the treatment of Parkinson's Disease is described. In addition, a method of improving cognition, speech and/or movement in a patient suffering from Parkinson's Disease comprising administering to the patient carbidopa, levodopa and trans-resveratrol is described.
EP1581198A1 Powdered medicament for inhalation comprising a tiotropium salt and salmeterol xinafoate The invention relates to powdered compositions for inhalation comprising a tiotropium salt and salmeterol xinafoate, a method for production and use thereof for the production of a medicament for treatment of respiratory diseases, in particular for the treatment of COPD (Chronic Obstructive Pulmonary Disease) and asthma.
WO2013013817A1 Substituted heterocyclic aza derivatives The invention relates to heterocyclic aza derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
US20120238628 Dihydronaphthalene and naphthalene derivatives as n-formyl peptide receptor like-1 (fprl-1) receptor modulators The present invention relates to novel dihydronaphthalene and naphthalene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
WO2002069885A9 Anti-invasive and anti-angiogenic compositions and methods for treating brain tumors and other diseases A peptide compound having the sequence Lys-Pro-Ser-Ser-Pro-Pro-Glu-Glu [SEQ ID NO:2] or a substitution variant, addition variant or other chemical derivative thereof inhibits cell invasion, endothelial tube formation or angiogenesis in vitro . A number of substitution variants and addition variants of this peptide, preferably capped at the N- and C-termini, as well as peptidomimetic derivatives, are useful for treating diseases and conditions mediated by undesired and uncontrolled cell invasion and/or angiogenesis. Pharmaceutical compositions comprising the above peptides and derivatives are administered to subjects in need of such treatment in a dosage sufficient to inhibit invasion and/or angiogenesis . The disclosed compositions and methods are useful for suppressing the growth and metastasis of tumors, including a number of highly malignant brain tumors, and for treating endometriosis and diseases associated with pathogenic neovascularization including various ocular diseases.
EP0869968B1 Growth-hormone secretagogues This invention is directed to compounds of formula (I) and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretagogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of formula (I).
CN102846868A Application of tibetan medicine RENQINGMANGJUE in preparing antitumor drug The invention discloses a new application of tibetan medicine RENQINGMANGJUE in preparing antitumor drug. The single RENQINGMANGJUE or combined application with chemotherapeutics has obvious antitumor effect, can improve immunologic function and protect thymus and spleen, and has synergism to chemotherapeutics.
EP2769717A1 A composition comprising reduced glutathione and acetaminophen and preparation method thereof The invention relates to a pharmaceutical composition of glutathione and acetaminophen and preparation method thereof. The active ingredients of the composition include glutathione with composition ration of 0.1% ∼ 99.9% and acetaminophen with composition ratio of 99.9% ∼ 0.1%. The further purpose of the invention is to prepare glutathione and acetaminophen composition (raw materials) into various pharmaceutically acceptable dosage forms, such as tablets, sustained/controlled release preparations, capsules, pills, syrups, films, granules, oral solutions, oral suspensions, oral emulsions and oral powders. The beneficial effects of the invention is reflected in that glutathione and acetaminophen combination can effectively prevent the liver cell damage and necrosis caused by acetaminophen overdose and is strongly in favor of cancer pain relieving and chemotherapy.
CN102908317A Macrolide antibiotics enteric-coated pellets and coating solution thereof The invention provides macrolide antibiotics enteric-coated pellets. The pellets are prepared by using a boiling pellet coating machine. The enteric coating solution is composed of a polyacrylic resin II, diethyl phthalate, Tween-80 and an ethanol solution. Besides, the invention provides a process and intermediate materials for preparing the macrolide antibiotics enteric-coated pellets, such as the coating solution and the like.
US7250424 Fab I inhibitors Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.
WO2013192229A1 Substituted pyridine azolopyrimidine - 5 - (6h) - one compounds Described herein are compounds and chemical entities of Formula I, methods of their synthesis, compositions comprising them, and their use in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders
CN102652740A Rupatadine fumarate dry powder inhalation and preparation method thereof The invention relates to the technical field of biological medication, and in particular relates to a repatadine fumarate dry powder inhalation and a preparation method thereof. The inhalation comprises repatadine fumarate serving as a main drug, as well as cystoid nasal dry powder inhalation with certain dosage of medicinal grains. The repatadine fumarate dry powder inhalation is used for treating allergic rhinitis, the medicament is inhaled into the nasal cavity, and can play local or whole body effect after being absorbed through nasal mucosa, and the medicament is taken in a cystoid mode, so that the dosage is accurate, and the risk of overdose does not exist; the medicament has quick absorption and quick response, can quickly enter into body circulation to achieve the aim of local and/or whole body treatment; and the patient has good compliance, so that the inhalation is particularly suitable for patients requiring long-term administration treatment.
CN103381272A Method for improving levodropropizine taste by cyclodextrin clathration The invention discloses a method for improving a levodropropizine taste by cyclodextrin clathration. The method comprises that cyclodextrin or cyclodextrin derivatives as carriers are added into levodropropizine so that levodropropizine is included in the cavity of the cyclodextrin or cyclodextrin derivatives and thus a levodropropizine clathrate is obtained. In oral administration, levodropropizine does not contact with the oral cavity of a patient so that the patient does not feel a peculiar smell and a bitter taste of levodropropizine. Therefore, the method effectively improves a levodropropizine taste and patient compliance, can prepare the levodropropizine solid dispersoid of which levodropropizine effects are not influenced, and can effectively improve clinical application of levodropropizine.
CN102988723A Preparation method and application of yin tonifying and calming tablet The invention provides a preparation method of a yin tonifying and calming tablet, which is prepared from crude drugs including 75g of angelica sinensis, 57g of radix ophiopogonis, 48g of schisandra chinensis, 39g of vine of multiflower knotweed, 39g of rhizome rehmanniae, 75g of poria cocos, 18g of platycladi seed, 75g of codonopsis pilosula, 93g of concha margaritiferausta, 57g of radix scrophulariae, 57g of salvia miltiorrhiza, 39g of polygala tenuifolia, 39g of platycodon grandiflorum and 10.2g of cinnabar through supercritical extraction and microwave extraction, so that the content of ferulic acid is greatly improved. The invention also provides the application of the yin tonifying and calming tablet in preparing a medicine for restraining proliferation of mice leukemia cell, L1210 cell.
US20080275114 Benzenesulfonamide derivatives; irritable bowel syndrome; may be co-administered with drug for inflammatory bowel disease; chemokine receptor inhibitors; Compounds of formula (I), in which R1 and R2 are independently a substituted phenyl group, where the substituents are as defined in the claims and with the proviso that at least one of the substituents is a cyano, carboxy or (C1-4)alkoxycarbonyl group, are inhibitors of CCR9 activity useful for therapeutic treatment, particularly of irritable bowel disease.
CN1631364A Application of tanshinone óÄA in pharmacy The invention relates to the use of tanshinone IIA in the preparation of medicaments for treating atherosclerosis, myocardial infarction, coronary heart disease, tumor, purulency osteomyelitis and tonsillitis. The tanshinone IIA of the invention can be prepared into various dosage types.
CN101503441A Nucleic acid molecule SI-CYPJ-1 and use thereof in anti-cancer medicine preparation The invention belongs to the biological medicine field, relating to nucleotide molecules and the application thereof in the preparation of antitumor medicines. The invention provides the nucleotide molecules for preparing the antitumor medicines. The nucleotide molecules have the activity for inhibiting the tumor growth and the sequence thereof comprises 5'GGAAGAGGAGGCAACAG-3' or 5'-CTGGAAGAGGAGGCAACAG-3'which is known as SI-CYPJ-1 in the invention. The nucleotide molecules SI-CYPJ-1 can obviously inhibit the tumor cell proliferation; when the nucleotide molecules are applied to a naked mouse, the tumor body growth of the naked mouse is obviously inhibited compared with the control naked mouse in the same condition of culture, and the phenomenon becomes obvious day by day as time goes on. The invention provides a new approach and means for the tumor treatment and mitigation.
US7790738 Methods of treating and preventing AIDS using of COX-2 inhibitors The present invention provides a method of treating or preventing a disorder typified by an immunodificiency (e.g. HIV), wherein the patient is administered a COX-2 inhibitor or derivative or pharmaceutically acceptable salt thereof, preferably diisopropylfluorophasphate. L-745337, rofecoxib, NS 398, SC 58125, etodolac, meloxicam, celecoxib or nimesulide, and compositions and products containing the same or use of the same in preparing medicaments and for treatment.
US20100227829 Motilide polymorphs The invention provides polymorphs of a motilide having a structure represented by formula Ia
US20060014683 Procoagulant protein comprising polypeptide with amino acid substitutions; resistant to activated protein C; von Willebrand factor binding site deleted and thrombin cleavage site is mutated; treating hemophilia The present invention provides novel purified and isolated nucleic acid sequences encoding procoagulant-active FVIII proteins. The nucleic acid sequences of the present invention encode amino acid sequences corresponding to known human FVIII sequences, wherein residue Phe309 is mutated. The nucleic acid sequences of the present invention also encode amino acid sequences corresponding to known human FVIII sequences, wherein the APC cleavage sites, Arg336 and Ile562, are mutated. The nucleic acid sequences of the present invention further encode amino acid sequences corresponding to known human FVIII sequences, wherein the B-domain is deleted, the von Willebrand factor binding site is deleted, a thrombin cleavage site is mutated and an amino acid sequence spacer is inserted between the A2- and A3-domains. Methods of producing the FVIII proteins of the invention, nucleotide sequences encoding such proteins, pharmaceutical compositions containing the nucleotide sequences or proteins, as well as methods of treating patients suffering from hemophilia, are also provided.
US20060148901 Acylated 4-amidino-and-4-guanidinobenzylamines for inhibition of plasma kallikrein The invention relates to the use of acylated 4-amidino- or 4-guanidinobenzylamine in accordance with the general formula I P4-P3-P2-P1 (I), where P4 is a monosubstituted or polysubstituted or unsubstituted benzylsulfonyl group, P3 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural α-amino acid or α-imino acid in the D configuration, P2 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural α-amino acid or α-imino acid in the L configuration, and P1 is a monosubstituted or polysubstituted or unsubstituted 4-amidino- or 4-guanidinobenzylamine group, for inhibiting plasma kallikrein (PK), factor XIa and factor XIIa, in particular for preventing the activation of coagulation at synthetic surfaces and for systemic administration as anticoagulants/-antithrombotic agents, in particular for preventing the activation of coagulation at synthetic surfaces for the purpose of averting thromboembolic events.
CA2573879A1 Anti-diarrhea preparations for small domestic animals A composition and method for treating diarrhea in small domestic animals wherein the composition includes an effective amount of kaolin, pectin, at least one probiotic, and a carrier, and the method includes the step of orally administering an effective dosage of the composition to the domestic animals.
US20080255244 CaM Kinase II Inhibitor Improves Retinoic Acid Therapy and Inhibits the Proliferation of Myeloid Leukemia Cells A method of treating a cancer (e.g., myeloid leukemia) in a subject in need thereof, is carried out by administering the subject a CaM kinase II (CaMK II) inhibitor. In some embodiments, the CaMK II inhibitor is administered concurrently with a retinoid. In some embodiments, the CaMK II inhibitor is CaMK II gamma inhibitor. Compositions and formulations useful for carrying out such methods are also described.
WO2007033475A1 THE USE OF siRNAs IN ORGAN STORAGE/REPERFUSION SOLUTIONS The invention is the modification of organs, tissues and cells with a storage/reperfusion solution comprising siRNAs specific for genes whose expression is associated with loss of viability or cell damage. The presence of siRNAs in the storage/reperfusion solution minimizes and/or prevents organ, tissue and cell damage such that the organs, tissues or cells can be used for in vivo transplantation. The invention is also directed generally to methods for maintaining organs, tissues and cells in a viable state using the storage/reperfusion solution.
WO2008089310A2 Delta 5 desaturase inhibitors for the treatment of obesity This invention relates to methods of treating, managing and preventing body composition disorders, and to compounds and pharmaceutical compositions useful in such methods.
WO2013005226A1 A novel combined pharmaceutical composition containing diclofenac and methods of making and using the same The present invention related to a synergistic pharmaceutical composition which contains more than one active ingredients which are diclofenac, glycofurol and Drotaverine with pharmaceutically accepted excipients. The present stable and effective combined composition shows enhanced efficacy and synergistic effect to provide protection from Dysmenorrhea, Gastrointestinal colic, Biliary colic, Renal colic, Dysmenorrheal and Abdominal pain associated with irritable bowel syndrome, Pre and Post lithotripsy, Post surgical smooth muscle spasm, Post-MTP (Medical termination of pregnancy) and D&C Dilatation and curettage thereof.
WO2013108857A1 Heterocyclic amide derivative and pharmaceutical product containing same A purpose of the present invention is to provide a novel compound which has TRPA1 antagonist activity and a pharmaceutical product which contains the compound. Another purpose of the present invention is to provide a TRPA1 antagonist and a medical agent which is useful for prophylaxis or treatment of diseases associated with TRPA1. A pharmaceutical product or the like which contains a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. (In formula (I), the symbols are as defined in the description.)
CN101890172B Application of S100A16 gene in preparing drug for treating obesity The invention relates to an S100A16 gene and an application of relevant access in developing a drug for treating metabolic disease. The invention provides a new gene relevant to obesity, provides a basis for research of molecular mechanism of obesity, reveals the important function of the S100A16 in obesity for the first time through construction of cell and animal model, provides a theoretical basis and feasibility in developing new drugs for treating obesity through research of S100A16 interacted protein and upstream-downstream gene on a signal access, and can be used as a new drug target.
EP2142524A1 Novel 5-cyano-prostacyclin derivatives and their use as agents for the treatment of influenza a viral infection This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1 - R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating respiratory diseases associated with influenza A viruses, such as for example H5N1and its mutations. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
US20060167005 New therapeutic uses of (4-(2-fluorophenyl)-6-methyl-2-(1-piperazinyl) thieno [2,3-d] pyrimidine (4-(2-Fluorophenyl)-6-Methyl-2-(1-Piperazinyl)Thieno[2,3-D]Pyrimidine or a salt thereof has value in the treatment of fibromyalgia, obesity, weight gain and other conditions.
CN102416165B Aerosol inhalation agent containing interferon alpha and dexamethasone sodium phosphate The invention belongs to the field of compositions of antiviral medicaments, and relates to an aerosol inhalation agent containing an interferon alpha and dexamethasone sodium phosphate. The aerosol inhalation agent contains a therapeutically effective amount of interferon alpha, dexamethasone sodium phosphate and an appropriate amount of pharmaceutically acceptable auxiliary materials; preferably, a single administration dose contains 2.5-30 mug of interferon alpha, 1-4 mg of dexamethasone sodium phosphate and an appropriate amount of pharmaceutically acceptable auxiliary materials; and morepreferably, a single administration dose contains 10-20 mug of interferon alpha, 2-3 mg of dexamethasone sodium phosphate and an appropriate amount of pharmaceutically acceptable auxiliary materials.When the aerosol inhalation agent containing the interferon alpha and dexamethasone sodium phosphate disclosed by the invention is used for treating viral pneumonia, the treatment effect is remarkably improved in comparison to separate use of the interferon alpha or the dexamethasone sodium phosphate.
WO2007023931A1 Composition for prevention of increase in blood alcohol level Pharmaceutical compositions, functional foods and the like are demanded which can prevent the increase in blood alcohol level after drinking to reduce the drunken degree and provide a comfortable drunken state so as to enjoy a moderate drunkenness. Thus, provided is a composition capable of preventing the increase in blood alcohol level. The composition comprises a basic amino acid (e.g., ornithine, arginine, lysine, histidine, citrulline) or a salt thereof as an active ingredient.
WO2013029525A1 Pharmaceutical composition comprising iodine polymer and glucocorticosteroid for treating dermatitis A pharmaceutical composition for treating dermatitis consists of 0.01% - 5% of povidone-iodine, 0.01% - 0% of glucocorticosteroid, 0.001% - 0.5% of potassium iodate and the rest of pharmaceutical acceptable carriers, wherein the glucocorticosteroid is propionate or halometasone.
CA2371583C Piperazine derivatives useful as ccr5 antagonists The use of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
US20060223811 Triglycerine depressant composition A blood triglyceride depressant composition which comprises pravastatin and one or more members selected from the group consisting of (1) pantethine, (2) inositol hexanicotinate, (3) a combination drug containing a riboflavin compound, a tocopherol compound and an ascorbic acid compound, and (4) a combination drug containing a tocopherol compound and an ascorbic acid compound.
WO2012020130A1 Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
CN101991530A Vinpocetine containing high-capacity sodium chloride injection and preparation method thereof The invention provides a vinpocetin containing high-capacity sodium chloride injection and a preparation method thereof, aiming at solving the problems that vinpocetin is mainly applied to middle aged and elderly patients, high-capacity glucose injection contains massive glucose and is not beneficial to treating patients suffering from diabetes at the same time. The invention has the key point that the injection is mainly composed of vinpocetin, osmotic pressure regulator, cosolvent and pH value regulator. The vinpocetin high-capacity sodium chloride injection of the invention has high bioavailability and stable quality, is convenient to use and is applicable to treatment of patients suffering from neurologic disease caused by cerebral circulation restriction, especially the patients suffering from diabetes at the same time.
CN102438611A Use of a combination of d-aspartic and l-aspartic acids or salts thereof for the treatment of male infertility The present invention concerns the use of a combination consisting of D-aspartic and L-aspartic acids or L-aspartic acid used alone to stimulate the procreative activity in the man by increment of spermatozoon number and motility.
US20080234243 Method of treating amyloidosis mediated diseases The compounds of the present invention can be used to inhibit formation of beta-amyloid protein. The present invention provides methods of preventing, delaying onset of, or treating diseases or conditions characterized or mediated by amyloidosis. In particular, the present invention is useful for preventing, delaying onset of, and treating Alzheimer's disease and related diseases causing dementia.
US20070265245 S-Mirtazapine For The Treatment Of Hot Flush The invention provides a method of treatment of hot flush with S-mirtazapine and the use of S-mirtazapine for the manufacture of a medicament for the treatment of hot flush.
CN103386119A Application of SIRT1 in adjusting rhythm and improving rhythm disorder The invention relates to an application of SIRT1 in adjusting rhythm and improving rhythm disorder. Specifically, the invention provides a method for adjusting the rhythm by using a SIRT1 protein, or an activating agent thereof, or an agonist thereof, or an antagonist thereof, particularly a method for improving rhythm disorder-related diseases by using the SIRT1 protein or the activating agent thereof. The invention also provides an application of the SIRT1 protein or the activating agent thereof in preventing and/or treating metabolic diseases such as 2-type diabetes, hypercholesteremia and the like which are resulted from the rhythm disorder. Experiments show that activating or up-regulating SIRT1 is helpful for improving the rhythm, reducing insulin resistance and improving hypercholesteremia.
WO2007119367A1 Composition containing biopterin and method for using the same Tetrahydrobiopterin (BH4) to be used as a pharmaceutical has an excellent efficacy, therefore, expansion of use or application thereof is considered. However, because BH4 is expensive and unstable to oxidation, its application to other than pharmaceuticals is difficult. Further, because BH4 is difficult to cross the blood-brain barrier, it is difficult to increase the brain level thereof in the current situation. The present inventors found that an effect equal or superior to BH4 can be expected by administering biopterin, an oxidized form of BH4, which is stable to oxidation, easy to handle and can be produced at a low cost. From this result, it was revealed for the first time that BH4 level in vivo (particularly, BH4 level in the brain which was difficult by BH4 administration) can be increased by administering a composition containing biopterin thereby to allow BH4 to act effectively.
US20050032753 Substituted phenol compounds useful for anesthesia and sedation The invention provides substituted phenol compounds and pharmaceutical compositions containing substituted phenol compounds which are useful for inducing or maintaining anesthesia or sedation in a mammal. This invention also provides methods for inducing or maintaining anesthesia or sedation in a mammal using substituted phenol compounds.
US20080004330 Aminomethyl-Azacycle Derivatives as Inhibitors of Monoamine Uptake The present invention provides compounds of formula (I) wherein A is (1), (2), (3), (4), (5), (6) or (7) and wherein R1, R7, y and Ar1 are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.
CN101829089A Application of ring B ethyoxyl silybin in preparing medicaments for treating viral hepatitis B The invention relates to application of ring B ethyoxyl silybin in preparing medicaments for treating viral hepatitis B, in particular to application of ring B ethyoxyl substituted silybin ester or a pharmaceutically acceptable salt thereof in preparing medicaments for clearing away HBsAG (Hepatitis B Surface Antigen) and HBeAg (Hepatitis B e Antigen) and suppressing the HBV (Hepatitis B Virus) DNA replication. The compound has strong activity on suppressing the HBsAG and the HBeAg, and in the presence of a concentration of 20 micrograms/milliliter, the intensities for clearing the HBsAg and the HBeAg are respectively 64.6 percent and 44.8 percent which are 4.0 times and 2.7 times of that of alpha-interferon which is a positive control medicament. In the presence of the concentration, the suppression rate of the compound on the HBV DNA is 58.1 percent which is 1.5 times of the corresponding activity of the alpha-interferon. Accordingly, the flavonolignan or the pharmaceutically acceptable salt thereof are indicated to simultaneously have strong efficacy on suppressing the HBsAg, the HBeAg and the HBV DNA and can be expected to be used for preparing non-nucleoside medicaments for treating HBV infection diseases.
CA2596015A1 Fused heterocyclic compounds useful as inhibitors of histone deacetylase Disclosed are compounds of formula (I) that inhibit histone deacetylase (HDAC) enzymatic activity, pharmaceutical compositions comprising such compounds, as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC, wherein A, W, W1, W2, Ar2, and G are described herein.
CN103191163A Skin wound repairing pharmaceutical composition The invention discloses a skin wound repairing pharmaceutical composition, and belongs to the field of medicines. The pharmaceutical composition comprises policresulen and centella triterpenes in an optimized weight ratio of (0.1-0.6):(0.01-0.5). The invention further provides gels, liniments, ointment, electuary or other external preparations prepared from the pharmaceutical composition for treatment of skin wound repairing. The pharmaceutical composition can be used for accelerating repairing and regeneration of wound tissues, promoting healing and reducing scar formation, thus the skin wound repairing pharmaceutical composition has wide medical application prospect.
WO2013175053A1 Catechol o-methyltransferase activity inhibiting compounds Compounds of formula (I), wherein R1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.
CN101307025B Chuanxiong alcohol carnitine ester compounds The invention discloses a rhizoma ligustici wallichii ethanol kearny ester compound capable of protecting cells and curing CCVD.
WO2008019048A1 Use of aromatase inhibitors for thining the endometrium or treating menorrhagia The invention provides a method of thinning the endometrium in a woman by utilizing a therapeutically effective amount of an aromatase inhibitor.
US20100069389 Novel forms of reboxetine The invention relates to novel crystalline forms of (2R)-2-[(R)-(2-ethoxyphenoxy)-phenylmethyl]morpholine hydrochloride. In various embodiments, the novel crystalline forms may be substantially enantiopure. The preparation and characterization of the novel crystalline forms of (2R)-2-[(R)-(2-ethoxyphenoxy)-phenylmethyl]morpholine hydrochloride is also described. The invention also relates to pharmaceutical compositions containing novel crystalline forms of (2R)-2-[(R)-(2-ethoxyphenoxy)-phenylmethyl]morpholine hydrochloride, which are useful to treat and/or prevent various conditions such as nervous system and pain disorders.
US20090306198 Anti-Oxidant Synergy Formulation Nanoemulsions to Treat Caner A uniform microfluidized nanoemulsion is disclosed containing a synergistic combination of two antioxidants and a cell membrane stabilizer phospholipid (i.e., an anti-oxidant synergy formulation; ASF). The microfluidized nanoemulsion improves the combination's cell membrane permeability by at least four-fold over conventional nanoemulsion compositions, which significantly increases the intracellular concentration of typically cell-impermeant antioxidants (i.e., for example, tocopherol) and/or systemic bioavailability. As a nanoemulsion, synergistic combination has greater anticancer efficacy than the same combination applied as a free solution.
US8043612 Infection and treatment of neoplasms with vesicular stomatitis virus The subject invention relates to viruses that are able to replicate and thereby kill neoplastic cells with a deficiency in the IFN-mediated antiviral response, and their use in treating neoplastic disease including cancer and large tumors. RNA and DNA viruses are useful in this regard. The invention also relates to methods for the selection, design, purification and use of such viruses for cancer therapy.
CA2292378C A method of inhibiting cancer cell growth using a vector expressing prb2/p130 Methods of inhibiting growth of cancer cells and treating cancer in a patient by administration of a vector expressing pRb2/p130 are provided.
US7381729 Gastrointestinal fluid solubility; adenosine-1 receptor agonist; hypertension, congestive heart failure, renal failure The present invention relates to the novel compound 4-(4-trans-hydroxycyclohexyl)amino-2-phenyl-7H-pyrrolo[2,3d]pyrimidine hydrogen mesylate, the polymorphic α and β forms thereof, and a method for the production of said compounds.
US20120178736 Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is 0, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
WO2009076200A3 Solid forms of 1-ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)-1h-benzo[d]imidazol-2-yl)urea Solid forms of crystalline1-ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)- 1H-benzo[d]imidazol-2-yl)urea, compositions containing solid forms of crystalline 1- ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)-1H-benzo[d]imidazol-2-yl)urea and methods of using the same are described.
USRE41149 Optically active pyridonecarboxylic acid derivatives N1-(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: These compounds have patent antibacterial activities against a wide variety of infectious bacteria and are useful as antibacterial agents by oral or parenteral administration.
US20120195933 Pharmaceutical compositions comprising tasocitinib The invention relates to pharmaceutical compositions, preferably tablets, comprising tasocitinib, suitable for immediate release, and processes of preparing such compositions.
CN1739543A Intravenous injection of antitumor compound nobiliside A and monoacetylated liposome and its prepn The present invention relates to medicine technology, and is one kind of intravenous liposome injection prepared with antitumor compound monoacetylated nobiliside A. The chemical structure of monoacetylated nobiliside A is shown, and pharmacological experiment shows that the intravenous liposome injection prepared with antitumor compound monoacetylated nobiliside A has obvious growth inhibiting effect on mouse H22 liver cancer, mouse S-180 sarcoma, human gastric carcinoma MGC803 and mouse transplanted tumor.
CN102091321A Medicament oral liquid for treating enteritis and diarrhea and preparation method thereof The invention relates to medicament oral liquid for treating enteritis and diarrhea. Raw medicines in the medicament oral liquid comprise the following components in parts by weight: 10-30 parts of poplar flower, 10-30 parts of echinacea, 10-30 parts of bee glue, 1-2 parts of muramyl dipeptide, 0.5-1 part of scopolamine methylbromide and 5-10 parts of D-mannose. The invention can effectively improve immunity, has good sterilizing and diarrhea relieving effect, lower cost and high killing rate on bacterium and virus pathogenic microorganisms, has no toxic or side effect and no medicine resistance, can not generate medicament residual and is convenient for use.
CN102008495A Application of berberine and doxorubicine mixed preparation in preparation of medicament against doxorubicine cardiac dysfunction or tumor The invention discloses application of a berberine and doxorubicine mixed preparation in preparation of a medicament against doxorubicine cardiac dysfunction or tumor. The molar concentration ratio of the berberine to the doxorubicine in the medicament is (0.625-4): 1, and the optimal ratio is 1:1. The medicament is an oral preparation or an injection preparation. The combined use of the berberine and the doxorubicine can lighten myocardial damage caused by the doxorubicine, also can play a role in inhibiting myocardial apoptosis caused by the doxorubicine, and does not weaken, even enhance the anti-tumor effect of the doxorubicine at the same time.
CN101040935A Dropping pills agent for removing phlegm and relieving asthma and cough and the preparing method The invention provides a dripping pill preparation for removing phlegm and relieving cough, which mainly comprises root of ballon flower, caffeine, polygala root, boneol, bitter apricot seed, Chinese gall and licorice root. The invention also provides the process for preparing the dripping pill preparation.
US7569387 Specifically binds an MK61 polypeptide produced by immunizing an animal Novel MK61 polypeptides and nucleic acid molecules encoding the same. The invention also provides vectors, host cells, selective binding agents, and methods for producing MK61 polypeptides. Also provided for are methods for the treatment, diagnosis, amelioration, or prevention of diseases with MK61 polypeptides.
CN101279966A Optical isomer of Nipradilol, preparation and medical use thereof Disclosed is an optical isomer of nipradilol, with the structural formula as showed in the right. The preparation method of the optical isomer including the following steps: condensing the material (3R)-3,4-dihydro-8-hydroxyl-3- nitro-oxyl-2H-1-chromene or the derivative thereof at 8-hydroxyl with R-epihydric alcohol or the derivative thereof; processing with isopropyl-amine. The optical isomer is capable of reducing intraocular pressure and can be applied to cure ocular hypertension and glaucoma.
WO2007023880A1 Chemokine production inhibitor A chemokine production inhibitor comprising a substance capable of inhibiting the function involved in signal transduction of GPR4 as an active ingredient; a chemokine production inhibitor comprising a nitrogenated tricyclic compound represented by the formula (I) or a quaternary ammonium salt or pharmacologically acceptable salt thereof as an active ingredient; and others: [Chemical formula] (I) wherein R1 represents a substituted or unsubstituted heterocyclic group, -NR5aR5b where R5a and R5b independently represent a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like) or the like; R2 represents a hydrogen atom or the like; R3 and R4 independently represent a hydrogen atom or the like; n represents 0 or 1; X represents -(CH2)2 or the like; and Y represents the following formula: [Chemical formula] where Z represents CH or a nitrogen atom; R8a and R8b independently represent a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; and R9 represents a hydrogen atom or the like.
WO2008039514A1 Pharmaceutical compositions and methods for treating diseases associated with neurodegeneration The present invention relates to methods for treating diseases, conditions or disorders using hydroxyamine compounds, and in particular, N-[2-hydroxy-3- (1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl chloride (Compound I) alone or in combination with one or more other therapeutic agents for the treatment of conditions, disorders or diseases associated with neurodegeneration in the central nervous system. Additional therapeutic agents are provided.The present invention also relates to pharmaceutical compositions comprising hydroxyamine compounds, an additional therapeutic agent and a pharmaceutically acceptable carrier and methods for treating diseases using them.
US20090041843 Pharmaceutical preparation having excellent photostability The present invention relates to a pharmaceutical preparation of high photostability which contains pitavastatin, which is an HMG-CoA reductase inhibitor, a salt of pitavastatin, or an ester of pitavastatin. The pharmaceutical preparation contains a pitavastatin compound, titanium oxide, and a colorant having a maximum absorption wavelength of 400 nm to 500 nm.
US20120022131 Breast cancer related gene rqcd1 The present invention provides methods for detecting and diagnosing cancer, such methods involving the determination of the expression level of the RQCD1, GIGYF1 or GIGYF2 genes. These genes were discovered to discriminate cancer cells from normal cells. Furthermore, the present invention provides methods of screening for therapeutic agents useful in the treatment of cancer and methods for treating cancer. Moreover, the present invention provides siRNAs targeting the RQCD1, GIGYF1 and/or GIGYF2 genes, all of which are suggested to be useful in the treatment of cancer.
US20090069381 Deuterium-enriched raloxifene The present application describes deuterium-enriched raloxifene, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN102001921A Sesquiterpene hybrid hydroquinone compounds and preparation method and application thereof The invention relates to a preparation method and application of two sesquiterpene hybrid hydroquinone compounds. The sesquiterpene hybrid hydroquinone compounds with novel structures are produced by adopting alternaria sp. SP-32 in a South China Sea sponge sample. Proved by experiments, the compounds have flu virus A H1N1 resistant effect, and have potential for developing flu virus A resistant medicament preparations.
CN103690592A Throat clearing and lung moistening composite The invention belongs to the field of health food, and relates to a method for processing a composite by taking a natural plant as a raw material, in particular to a throat clearing and lung moistening composite. The composite is processed by raw materials such as hylocereus undatus flower, sinopimelodendron kwangsiense, Chinese black olive, liquorice, momordica grosvenori and rock candy. The composite has good effects of clearing away heat and toxic materials, diminishing swelling, relieving a pain, clearing a throat, moistening a lung, relieving a cough, reducing sputum, clearing and relaxing bowels, preventing a cold, improving immunity, protecting health and the like, and has the characteristics of simple compatibility, easiness in raw material obtaining, diversified effect, safety, reliability, good taste, convenience in carrying, simplicity in taking and the like.
US20110318418 Compositions of 5-ethyl-2--pyrimidine This invention relates to the field of pharmaceutical chemistry and, more specifically, to pharmaceutical formulations as well as to intermediates used to prepare such formulations and to methods for manufacturing such formulations.
WO2007124625A1 Limax polysaccharides, the production process and the use of the same Limax polysaccharides, the production process and the use of the same. Limax polysaccharides are extracted from limax glycoprotein. The production process includes the steps of piecewise salting-out and Sevag removing-protein. Limax polysaccharides can be used for producing the medicines of treating lung cancer, bronchitis and asthma.
CN102949393A Medicine composition for curing liver damage The invention discloses a medicine composition for curing liver damage, which almost basically comprises lycopene and one of 1, 4, 5,6-tetrahydrogen-2-methyl-4-pyrimidinyl carboxylic acid, and 1,4,5,6- tetrahydrogen-2-methyl-5- hydroxyl-4--pyrimidinyl carboxylic acid, and lycopene. The composition which comprises the two components within a proportional range has a remarkable therapeutical effect to the liver damage caused by various reasons.
EP1767536B1 Quinolonecarboxylic acid compounds, preparation methods and pharmaceutical uses thereof The present invention has disclosed a kind of quinolone carboxylic acid derivatives, their pharmaceutically acceptable salts and hydrate, as well as their preparation process and medical usage. The compounds show powerful antibiosis activity to a wide spectrum of nosogenetic bacterial strains, display good property of pharmaceutical kinetics and are low in toxicity. There are hydrogen atom or amino at 5- position, cis-substituted optical rotation active or racemic 2, 8-diazobicycle [4, 3, 0]-nonyl at 7-position and difluoromethoxy at 8-position of the quinolone core of the quinolone compounds. Compared with those known quinolone antibiosis medicines, the inventive compounds have excellent antiGram-positive activity and a wide spectrum of antibiosis activity.
CN101697966A Application of furanodiene in preparation of medicaments for treating diseases caused by viruses The invention relates to new application of furanodiene in the field of pharmaceutics, in particular to application of furanodiene in the preparation of medicaments for treating the diseases caused by herpersvirs, influenza viruses and hepatitis B viruses.
US20080019979 HERV-K Antigens, Antibodies, and Methods Methods and compositions for cancer diagnostics and therapy are provided. More particular, methods and compositions for detecting, preventing, and treating HERV-K+ cancers are provided. One example of a method may involve a method for preventing or inhibiting cancer cell proliferation by administering to a subject a cancer cell proliferation blocking or reducing amount of a HERV-K env protein binding antibody.
US20100098786 Formulation containing a carboxylic acid or an ester thereof A formulation comprising eicosapentaenoic acid, or an ester thereof, and a triterpene, or an ester thereof, and the use of such a formulation.
WO2012069790A1 Therapeutic use of compounds A compound having the formula (I) R1 - COOH wherein R1 is an alkyl or alkenyl group having a C7-11 backbone, optionally branched with a C1-6 alkyl group at any C position in the backbone, or a pharmaceutically acceptable salt, amide or ester thereof, wherein the backbone of the alkyl or alkenyl group, and/or the branched alkyl groups, are optionally interrupted by one or more heteroatoms, provided that when R1 is an alkyl group having a C7 backbone, the branching does not consist only of a hexyl group at the a carbon of R1, or only of a methyl group at the γ carbon of R1, or of only single methyl groups at both the β and ω-1 carbons of R1, and provided that when R1 is an alkyl group having a C8 or C11 backbone, the branching does not consist only of a propyl group at the a carbon of R1, for use in the treatment or prevention of a disease or a biomedical condition selected from seizure-related disorders, bipolar disorders, mania, depression, migraine, attention deficit hyperactivity disorders, latent HIV infection, Alzheimer's disease, chorea, schizophrenia, ischemia, cancer and fatal blood loss.
US20100075969 Angiogenesis The invention provides medicaments comprising an agent, which selectively modulates β2-adrenergic receptor conformation, or receptor activity, or activation thereof. The medicaments may be used for treating diseases that are characterised by disorganized and/or abnormal vasculature, such as cancer and metastatic disease. The medicaments may also be used for promoting organized/normal branched vasculature.
CN102440991A Composition for treating duck scrositis and preparation method thereof The invention which discloses a composition for treating the duck scrositis and a preparation method thereof aims to provide a composition for treating the duck infection, reducing the medicine resistance probability of pathogens and improving the cure rate and a preparation method thereof. The composition comprises, by weight, 5-20% of thiamphenicol, 5-15% of norfloxacin nicotinate, 5-15% of taurine, and the balance waterless glucose. The combination of thiamphenicol and norfloxacin nicotinate adopted in the invention, which allows the medicine resistance of a Riemerella anatipestifer to be substantially reduced and the antipathogen resistance to be improved and has strong inhibiting and killing effects on other bacteria, can prevent the generation of the secondary infection of other bacteria. Taurine which has the antipyretic and anti-inflammatory functions can effectively and pertinently treat clinical symptoms caused by the duck scrositis, so the symptomatic treatment is realized. The duck scrositis infection is treated and the cure rate is improved through the reasonable combination match of above medicines in the invention.
US7176316 Amino-piperidine derivatives The present invention relates to compounds of the general formula wherein X and Y are each independently selected from —CH2— or —O—, with the proviso that X and Y are not simultaneously —O—; A is —S(O)2— or —C(O)—; and R1, R2, R3, and R4 are as defined in the specification. The compounds are GlyT-1 inhibitors and are useful for the treatment of psychoses, pain, dysfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
US7462631 e.g. 4-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-3-methyl-N-piperidin-1-ylthiophene-2-carboxamide; cannabinoid receptor antagonist; antiinflammatory agent; obesity, gastrointestinal disorders, inflammatory phenomena, immune system diseases, psychotic disorders, alcohol and nicotine dependence The invention discloses and claims a compound of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R11 are as defined herein. Further embodiments of the invention include a method of preparation of a compound of formula (I), its pharmaceutical composition and a method of treatment of a disease using a compound of formula (I).
WO2008003149A3 Substituted pteridines for the treatment and prevention of viral infections Tri-substituted pteridines and tetra-substituted pteridines exhibit a significant and selective activity against certain types of viral infections, in particular they selectively inhibit the replication of the hepatitis C virus, and are useful for the prevention and treatment of such infections.
US20090197937 Marine actinomycete taxon for drug and fermentation product discovery The invention is the discovery of an actinomycete genus, given the name Salinospora gen. nov., that displays an obligate requirement of seawater (Na+) for growth and unique 16S rRNA signature nucleotides. The invention is also the use of the genus for the production and discovery of active biomolecules such as pharmaceutical agents, agrichemicals, immunomodifiers, enzymes and enzyme inhibitors.
US20080317819 Iop lowering drug combination or non-combination loaded contact lens with zonal drug delivery areas A contact lens for delivery of a multiplicity of drugs includes a lens body with a first drug incorporated in a first zonal area of the lens body and a second drug incorporated in a second zonal area of the lens body. The first and second drugs are dissimilar and the first and second zonal areas are spaced apart from one another.
EP1640002A1 Indazole derivatives for inhibition of angiogenesis A method for inhibiting cell proliferation, cell migration, or tube formation induced by an angiogenic factor. The method includes administrating to a subject in need thereof an effective amount of a compound of the formula: wherein A is H or in which n is 0, 1, 2, or 3; each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR', (CH2)mOR, (CH2)mSR, (CH2)mNRR', (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH=NOR, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R', independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.
CN1749282A Belly bottom snail polysaccharide and its preparing method The present invention relates to polysaccharide matter, and is belly button snail polysaccharide of purity 25-55 % and produced with belly button snail meat and/or leftover, and through homogenizing, enzymolysis, water extracting, concentration, alcohol precipitation, eliminating protein, alcohol precipitation and freeze drying. The present invention also provides food composition with the belly button snail polysaccharide as active component. The present invention combines ultrasonic treatment, microwave treatment, enzymolysis and hot water lixiviating to extract the active components of belly button snail polysaccharide and has high polysaccharide yield. The belly button snail polysaccharide may be used in develop functional food with the functions of regulating immunity, resisting cancer and inhibiting tumor.
EP1941876A1 Isosorbide mononitrate derivatives for the treatment of Inflammation and ocular hypertension The present invention relates to the use of a compound of formula (I) or a tautomer, a pharmaceutically acceptable salt, a prodrug or a solvate thereof: as active ingredient(s) in the manufacture of a pharmaceutical composition for the prevention and/or treatment of an ophthalmological disease mediated by ocular hypertension and/or an intestinal disorder.
WO2012058719A1 Inhalable compositions There is described a composition for nebulisation comprising a non-ionic hyperosmolar agent and an electrolyte, wherein the electrolyte can include a sodium or potassium salt, and the electrolyte can include xylitol, mannitol, sorbitol or saccharin. Also described is a method of forming a nebulised composition and its use in the treatment of respiratory conditions such as cystic fibrosis, bronchiectasis or asthma.
CN102399213A Lamivudine monophthalate and synthetic method thereof The invention discloses a lamivudine monophthalate, a synthetic method thereof and a purpose thereof. The preparation method of the lamivudine monophthalate is simple, the salt forming yield is high, and a raw material phthalic acid is easily obtained and has small toxicity. The lamivudine monophthalate can be conveniently and efficiently separated from a polar solvent containing inorganic salts, and high purity lamivudine can be conveniently obtained by dissociating the lamivudine monophthalate. The lamivudine monophthalate is a pharmaceutically acceptable salt.
US20130225412 Silicon nanocarrier for delivery of drug, pesticides and herbicides , and for waste water treatment The various embodiments herein provide a nano silicon carrier as a drug delivery mechanism. The nano silicon carrier comprises a diatom frustules loaded with a drug molecule to be released at the target site. The diatom frustules are of Hannaea arcus and Navicula inflexa species of diatom. The pore size of the diatom frustules is 1 to 100 nm. The diatom frustules are comb-like in structure. The diatom frustules are in the form of powdered diatomaceous earth. The drug delivery mechanism described in the embodiments herein is a controlled release mechanism. The nano silicon carrier described in the embodiments herein is also used for delivery of pesticides and herbicides in plants. The nano silicon carrier described in the embodiments herein is also used in hormone waste water treatment.
EP1594833B1 1-phenylalkanecarboxylic acid derivatives for the treatment of neurodegenerative diseases 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.
CN102451174A Application of protocatechualdehyde to preparation of medicaments for treating human neurodegenerative diseases The invention discloses application of protocatechualdehyde to preparation of medicaments for treating human neurodegenerative diseases. The invention first discovers that the protocatechualdehyde has activity of interacting with parkinsonism-related protein DJ-1 and further discovers that the protocatechualdehyde has the effects of resisting oxidative stress, preventing apoptosis of SH-SY5Y neurocyte, induced by the oxidative stress, restricting active oxygen in the neurocyte from generating, and the like through experiments. Proved by experimental results, the effect of the protocatechualdehyde to the neurocyte is mediated by the DJ-1 protein, and the protocatechualdehyde has an exact neuroprotective effect and can be used for preventing or treating the neurodegenerative diseases comprising parkinsonism.
CN1820738A Tramadol hydrochloride slow release dripping pill and its preparing method The present invention relates to pain relieving medicine preparation, and is especially one orally taken slow released preparation with tramadol hydrochloride as main material. The present invention provides slow released tramadol hydrochloride dripping pill superior to available technology. The slow released tramadol hydrochloride dripping pill has the advantages of controllable releasing period, complete medicine release and high bioavailability.
CN102844029A Beta-carbolines for use in the treatment of hearing loss and vertigo The invention relates to beta-carbolines, preferably 9-alkyl-beta-carbolines (9-alkyl-BC), the production thereof and the use for the prophylaxis and treatment of hearing loss, tinnitus, acoustic shocks, vertigo and equilibrium disorders and to pharmaceutical compositions containing said beta-carbolines.
CN101006977A Anticancer medicinal composition containing taxane and hormones drug Disclosed is a slow release injection agent of anticancer composition containing taxone and/or hormone medicaments, which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents selected from taxone and/or hormone medicaments and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP/TC), p(BHET-EOP/TC), p(BHDPT-EOP/TC), p(BHDPT-EOP/TC), p(CHDM-HOP) or p(CHDM-EOP), copolymer of polyphosphate ester with polylactic acid, Polifeprosan, di-aliphatic acid and sebacylic acid, copolymer or blend of poly(erucic aciddipolymer-sebacylic acid) or poly(fumaric acid-sebacylic acid). The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 40 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.
EP1723138B1 Substituted benzimidazoles and their use for inducing apoptosis The invention relates to compounds of formula (I), wherein R represents aryl or heteroaryl, X is a bond, a carbonyl group, a derivative of a carbonyl group, an ethylene group or an ethylenecarbonyl group, R1 is optionally substituted amino or hydroxy, and the substituents R2 to R6 have the meanings given in the specification, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to intermediates, to the use of a compounds of formula (I) as a medicament and for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.
CA2848351A1 Composition and dressing for wound treatment The invention provides methods and compositions for wound treatment and/or blood clot formation, e.g., arresting the flow of blood from an open wound. The methods and compositions provide for promoting and accelerating wound healing and optionally provide for inhibition of microbial infection and/or a local analgesic effect.
WO2014074670A1 ALKYL AMIDE-SUBSTITUTED PYRIMIDINE COMPOUNDS USEFUL IN THE MODULATION OF IL-12, IL-23 AND/OR IFNα Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition.
WO2012061958A1 Flavone derivatives and their preparative method and medical use The present invention provides flavone derivatives, preparative method of the derivatives and use thereof as medicaments for treating diabetes. The structure of the derivatives is presented by formula 1: In the structure, R1 and R2, which are identical or not, represent hydrogen atom, halogen, cyano, hydroxyl, trifluoromethyl, thio-methyl, benzyloxy, C1-C8 linear chain or branch chain alkyl, C1-C8 linear chain or branch chain alkoxy. The pharmacological test indicates that the flavone derivatives can significantly increase the glucose consumption of Hep-G2 cell with insulin resistance activity, promote translocation of glucose transporter 4 of skeletal muscle cells (L6GLUT4myc) at different level, and significantly increase glucose intake and utilization by cells. The test proves the fact for the first time that the flavone derivatives can significantly promote translocation of glucose transporter 4 of skeletal muscle cells, and one of the mechanisms for treating diabetes is activating the cell AMPK phosphorylation and phosphorylating the downstream ACC.
CN102046200A Therapeutic for hepatic cancer Provided are a novel medicinal composition for treating or preventing hepatocellular carcinoma and a therapy method. Disclosed is a medicinal composition for treating or preventing hepatic cancer which comprises a chemotherapeutic agent combined with glypican 3 antibody. Also disclosed are a medicinal composition to be used in combination with a chemotherapeutic agent for treating or preventing hepatic cancer which comprises glypican 3 antibody as the active ingredient; and a medicinal composition to be used in combination with glypican 3 antibody for treating or preventing hepatic cancer which comprises as the active ingredient a chemotherapeutic agent. The combined use of a chemotherapeutic agent with glypican 3 antibody can achieve better therapeutic effect than the chemotherapeutic agent employed alone. Moreover, side effects in treating hepatic caner with the use of the chemotherapeutic agent can be reduced thereby.
US20130039894 Polypeptides and Use Thereof for Treatment of Traumatic or Degenerative Neuronal Injury The present invention relates to polypeptides transiently activating Ras homolog gene family member A (RhoA) GTPase, polynucleotides encoding said polypeptides and pharmaceutical compositions comprising said polypeptides or said polynucleotides. The present invention further relates to the use of said polypeptides, said polynucleotides or said pharmaceutical compositions for long-term treatment of damage of the peripheral or central nervous system.
CN103370289A 4-hydroxybutyric acid deuterated analogs This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
EP1637143A1 Sulfacetamide formulations further containing a sunscreen for treatment of rosacea A method for treating rosacea in a patient comprising administering to a patient suffering from rosacea a first topical composition comprising at least one sulfacetamide or a derivative thereof and at least one sunscreen, wherein the administration of said first composition provides a more effective treatment of said rosacea in comparison to treatment of rosacea achieved by administration of a second topical composition comprising metronidazole.
US20110124726 Novel carboxylic acid derivatives The present invention is concerned with novel arylalkyl carboxylic acid derivatives, more specifically, with acylates of arylalkyl carboxylic acids with naturally occurring, non-toxic hydroxyl, sulfhydryl, amino or imino compounds, and to compositions containing them. The compositions are preferably cosmetic preparations.
US20130309325 Composition and method for promoting joint and bone health The present invention provides compositions comprising silicon and at least one other joint health ingredient such as glucosamine, chondroitin, hyaluronic acid, collage, etc. as well as methods for making and using the same.
US7572801 Pyridopyrimidinone derivatives which are HM74A agonists The invention is concerned with novel pyridopyrimidinone derivatives of formula (I): wherein R1 to R8, X, Y, m and n are as defined in the description and in the claims. The compounds of the present invention are HM74A agonists with improved properties compared to niacin and can be used for the treatment and/or prevention of diseases such as dyslipidemia, atherosclerosis, diabetes, metabolic syndrome, and other related diseases associated with HM74A.
CA2623813A1 Nitrogen-containing heterocyclic compound and pharmaceutical application thereof It is intended to provide a compound represented by the general formula (I): (I) (wherein all the symbols are as defined in the description) which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.
WO2007077508A2 Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors The present invention relates to β-amino acid derivatives as dipeptidyl peptidase- IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
CN102813909A Compound doxycycline hydrochloride composition for preventing and treating colibacillosis and chronic respiratory disease of poultry as well as preparation method thereof The invention relates to a compound doxycycline hydrochloride composition for preventing and treating colibacillosis and chronic respiratory disease of poultry as well as a preparation method of the compound doxycycline hydrochloride composition. The compound doxycycline hydrochloride composition is prepared by uniformly mixing the following components by weight: 10-15 parts of doxycycline hydrochloride, 10-20 parts of colistin sulfate, 5-15 parts of tylosin tartrate, 5-10 parts of trimethoprim lactate and 40-70 parts of anhydrous dextrose. The compound doxycycline hydrochloride composition has the beneficial effects of reasonable formula, easiness in preparation, remarkable treatment effect and clinically proven special effect for treating colibacillosis and chronic respiratory disease of the poultry.
US20110027194 Hypochlorite denture compositions and methods of use A solid composition including calcium and/or magnesium hypochlorite, a builder (e.g., one or more of carbonate, bicarbonate, sesquicarbonate), an acid, a water-soluble polymer, at least one anionic surfactant, and optionally, a hydrotrope. The composition does not include any potassium hypochlorite, sodium hypochlorite, lithium hypochlorite, N-halogenated compounds, peroxides, persulfates, hydantoins, isocyanurates, or carboxylic acids that also have hydroxyl, amino, amido, imino, or imido groups. Upon dissolution of the composition in water, the calcium and/or magnesium hypochlorite and acid react to form hypochlorous acid. The use of hypochlorous acid, rather than direct use of an alkaline or alkaline earth hypochlorite results in a composition that is typically acidic rather than basic, and that results in improved cleaning. The composition is particularly suited for cleaning and disinfecting dentures.
CN102872079A Application of Houttuynoid C in drugs for restraining multiplication of liver fibroblasts The invention relates to an application of Houttuynoid C in drugs for restraining multiplication of liver fibroblasts. A pharmacological test proves that Houttuynoid C can obviously restrain the occurrence and development of liver fibrosis and can be applied to preparing anti-liver fibrosis drugs and drugs for preventing and treating cirrhosis of liver. The application of Houttuynoid C in drugs for restraining multiplication of liver fibroblasts disclosed by the invention is publicized for the first time. The skeleton type is brand new and has an unexpectedly strong inhibitory activity to the multiplication of liver fibroblasts; the possibility for other compounds to give any inspiration does not exist; the application has outstanding substantial characteristics and is obviously a significant progress to the restraint of the multiplication of liver fibroblasts.
US20080267951 Methods for Treating Cancer Using Agents That Inhibit Wnt16 Signaling This invention relates to methods of inhibiting the growth of cells, in particular cancer cells that over express Wnt16 protein. The methods comprise contacting the cell with an agent that binds to Wnt16 mRNA or Wnt16 protein, interferes with Wnt16 signaling or inhibits binding of the Wnt16 protein to another protein, such as a Frizzled receptor.
WO2014048836A1 Stabilized aqueous compositions of neuromuscular blocking agents The present invention relates to an aqueous composition comprising: (i) a quaternary ammonium neuromuscular blocking agent; and (ii) an excipient selected from a polyhydroxy acid of the following formula: HO-CH2-[CH(OH)]n-COOH, wherein n is an integer from 1 to 8, an intramolecular lactone of said polyhydroxy acid or a mixture thereof. Furthermore the present invention relates to a liquid pharmaceutical composition comprising or consisting of said aqueous composition and a method for producing said aqueous composition comprising the steps of: a) providing a quaternary ammonium neuromuscular blocking agent wherein said quaternary ammonium neuromuscular blocking agent is optionally freeze-dried, b) providing an excipient selected from a polyhydroxy acid of the following formula: HO-CH2-[CH(OH)]n-COOH, wherein n is an integer from 1 to 8, an intramolecular lactone of said polyhydroxy acid or a mixture thereof, wherein said excipient is optionally freeze-dried, c) mixing the quaternary ammonium neuromuscular blocking agent of step a) and the excipient of step b) in water to give an aqueous composition. In addition, the present invention relates to the use of a polyhydroxy carboxylic acid of the following formula: HO-CH2-[CH(OH)]n-COOH, wherein n is an integer from 1 to 8, an intramolecular lactone of said polyhydroxy acid or a mixture thereof for stabilizing an aqueous composition comprising a quaternary ammonium neuromuscular blocking agent. The present invention also refers to a container containing the aqueous composition or the liquid pharmaceutical composition of the present invention. It furthermore relates to a kit comprising said compositions. Preferred embodiments are apparent from the dependent claims.
US20100257616 DNA regulatory element for the expression of transgenes in neurons of a subject and uses thereof The present invention provides for a recombinant nucleic acid molecule comprising a region of a calcium-calmodulin dependent kinase IIα promoter operatively linked to a gene of interest. The region of a calcium-calmodulin dependent kinase IIα promoter may comprise an 8.5 kilobase nucleic acid sequence which corresponds to the nucleic acid sequence of ATCC Accession No.: ______, designated pMM281. The present invention also provides a human cell line which has been stably transformed by a recombinant nucleic acid molecule comprising a gene of interest operatively linked to a nucleic acid encoding a calcium-calmodulin dependent kinase IIα promoter region which has a nucleotide sequence corresponding to the sequence of ATCC Accession No. ______, designated pMM281. The present invention also provides for a transgenic nonhuman mammal whose germ or somatic cells contain a nucleic acid molecule which encodes a gene of interest under the control of a CaMKIIα promoter (ATCC Accession No. ______), introduced into the mammal, or an ancestor thereof, at an embryonic stage. Another embodiment of the present invention is a method of evaluating whether a compound is effective in treating symptoms of a neurological disorder in a subject which comprises: (a) administering the compound to the transgenic nonhuman mammal whose germ or somatic cells contain a nucleic acid molecule which encodes a gene of interest under the control of a CaMKIIα promoter, and (b) comparing the neurological function the mammal in step (a) with neurological function of the transgenic mammal in the absence of the compound, thereby determining whether the compound is effective in treating symptoms of the neurological disorder in a subject.
CN102552124A Liquid medicine composition of Ramosetron The invention relates to a liquid medicine composition of Ramosetron. According to the invention, the liquid medicine composition comprises a curing and/or preventing effective quantity of Ramosetron or pharmaceutically acceptable salt, absorption enhancer and water thereof. The liquid medicine composition of the Ramosetron, provided by the invention, has the advantages as shown in the specification.
US20130005714 Water-Soluble Meloxicam Granules Water soluble meloxicam granules comprising: (a) meloxicam; (b) a salt forming agent which forms the meglumine, sodium, potassium, or ammonium salt of meloxicam; (c) a binder; (d) a sugar or sweetener; and (e) a carrier, and optionally a flavoring agent and optionally other excipients, processes for preparing them and their use for treating respiratory or inflammatory complaints in mammals.
WO2008056687A1 Novel spiropiperidine derivative [PROBLEMS] To provide a compound having excellent stearoyl-CoA-desaturase inhibitory activity or a pharmacologically acceptable salt thereof. [MEANS FOR SOLVING PROBLEMS] A compound having the general formula (I) or a pharmacologically acceptable salt thereof. (I) wherein A represents a group represented by the formula: -CONHR1 or -ER2 (wherein R1 represents a C1-C6 alkyl group which may be substituted by 1 to 5 groups independently selected from members of a substituent group “a”, or the like; E represents a 1,3,4-oxadiazole group, a 1,2,4-oxadiazole group or an imidazole group; and R2 represents a C1-C6 alkyl group substituted by 1 to 5 groups independently selected from members of a substituent group “a”, or the like); R3 represents a hydrogen atom or the like; R4 represents a hydrogen atom or the like; R5 represents a hydrogen atom or the like; R6 represents a hydrogen atom or the like; R7 represents a hydrogen atom or the like; R8 represents a hydrogen atom, a halogen atom or the like; Z represents a nitrogen atom or the like; Y represents a nitrogen atom or the like; U represents a singlebond, a methylene group or the like; Vrepresents a single bond, a methylene group or the like; W represents a methylene group, a group represented by the formula: -CH(OH)-, or the like; m represents a number of 0 or 1; n represents a number of 0 or 1; the substituent group “a” includes a halogen atom, a hydroxy group, and a C6-C10 aryl group which may be substituted by 1 to 5 groups independently selected from member of a substituent group “b”; and the substituent group “b” includes a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a hydroxyl group and the like.
EP1937272A2 Benzodiazepines as hcv inhibitors The present invention relates to the use of benzodiazepines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates Io benzodiazepine compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.
CN101618018B Miconazole nitrate particle, and preparation method and medicinal composition thereof The invention discloses a miconazole nitrate particle, and a preparation method and a medicinal composition thereof. The preparation method comprises the following steps: 1) adding miconazole nitrate into a solvent for heating and dissolution, wherein the solvent is alcohol-propylene glycol mixed solution or ethanol-glycerin mixed solution, and then filtering the obtained solution; 2) adding the filtrate obtained in the step 1) into purified water or water for injection at a temperature of 0 to 5 DEG C, stirring the water added with the filtrate, adding a deflocculant into the water added with the filtrate and stirring the solution added with the deflocculant to obtain a mixture of water and crystals; and 3) as usual, filtering the mixture of the water and the crystals obtained in the step 2), washing away the solvent from the crystals obtained by the filtering with the purified water or the water for injection and then vacuum-drying the obtained crystals in which the solvent is washed away. The invention sets a precedent of adopting micro-crystallization to configure an electrolyte neutralization process and a dual-solvent process in the preparation process for miconazole nitrateparticles, thereby developing a miconazole nitrate particle with strong controllability, convenient operation and higher quality, and a preparation method thereof.
US20050008568 Complex containing dithiocarbamate compound The invention relates to a technetium or rhenium complex of formula (I): [M (R1CS3)2L] (I) in which M is Tc or Re, R1 represents an alkyl, cycloalkyl, aralkyl or aryl group which is unsubstituted or substituted by one or more substituents chosen from halogen atoms, the hydroxyl group, alkyl groups and alkoxy groups, and L is a dithiolate ligand, with the exception of the ligand of formula R2CS2 in which R2 is identical to R1. The dithiolate ligand is preferably a dithiocarbamate. The invention also relates to a radiopharmaceutical product comprising a complex of formula (I) with M representing 99Tc, 186Re or 188Re.
CN1739534A Compound medicine prepn of ginseng stem and leaf total saponin and propolis total flavone for treating gastropathy The compound medicine preparation of ginseng stem and leaf total saponin and propolis total flavone for treating gastropathy is prepared with ginseng stem and leaf total saponin in 4-8 weight portions and propolis total flavone in 1 weight portions and through mixing and conventional pharmaceutical process. The medicine preparation may be used in preventing and treating gastric ulcer, acute and chronic gastritis duodenal ampulla ulcer, and other gastric diseases, owing to its pain relieving and inflammation diminishing effects.
WO2012034204A1 Pharmaceutical association for treating and/or preventing myoma and/or endometriosis, use of resveratrol and progestogen, pharmaceutical composition for treating and/or preventing myoma and/or endometriosis, medicament for treating and/or preventing myoma and/or endometriosis, kit and method for treating and/or preventing myoma and/or endometriosis The present invention relates to an association of resveratrol with progestogens, and to pharmaceutical compositions and medicaments containing same, useful for the treatment and/or prevention of myoma and/or endometriosis, reducing the dimensions thereof and controlling the associated symptoms. This association can additionally contain an estrogen component. Also disclosed are a method for treatment and a kit.
US7345040 Piperimido[1,2-a]piperazine-4,7diones derivatives; neurokinin (tachykinin) receptor antagonists; mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins; analgesic, neurodegenerative disorders, respiratory diseases, antiinflammatory agent, antidepressant Reverse-turn mimetics and methods relating to the same having the following structure are disclosed: including pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3 and R4 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are neurokinin (tachykinin) antagonists. Libraries containing the reverse-turn mimetics of this invention are also disclosed.
CN102311399A Triazole alcohol antifungal compounds with nitrogen-containing side chains, preparation method thereof and application thereof The invention relates to the technical field of medicines. Present antifungal medicines which have problems of large side effect, narrow antimicrobial spectrum, easy generation of the drug resistance and the like cannot satisfy clinical treatment needs. The invention provides novel triazole alcohol antifungal compounds with high efficiency, low toxicity and wide spectrum and pharmaceutically acceptable salts thereof. The compounds are 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(nitrogen-containing side chain substituted)-2-propanol compounds, and the general structure of the compounds is shown in the specification. The invention also provides a preparation method of the compounds and an application of the compounds in the preparation of antifungal medicines.
US20100298380 N-aryl-n-piperidin-4-ylmethyl-amide derivatives and thier use as monoamine neurotransmitter re-uptake inhibitors This invention relates to novel N-aryl-N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.
WO2013067682A1 A hydrocolloid composition and an article containing the same The present invention provides a hydrocolloid composition which, based on 100% by weight of the hydrocolloid composition, comprises: 10-90%) by weight of a polyisobutylene tackifier; 5-55% by weight of a hydrophilic absorbing substance; and 0.1-20% by weight of a functional ingredient. The invention further provides an article containing the hydrocolloid composition.
CN102718650A 2-(2- hydroxyl-5-(methoxycarbonyl) phenoxyl) benzoic acid as well as preparation method and application thereof The invention discloses 2-(2- hydroxyl-5-(methoxycarbonyl) phenoxyl) benzoic acid as well as a preparation method and an application thereof. The structural formula of the 2-(2- hydroxyl-5-(methoxycarbonyl) phenoxyl) benzoic acid is shown in a formula (I). A new 2-(2- hydroxyl-5-(methoxycarbonyl) phenoxyl) benzoic acid compound is prepared, separated and obtained from litchi pericarp and has good antioxidant activity, and the antioxidant activity of the compound is remarkably stronger than that of a synthetic antioxidant BHT (Butylated Hydroxytoluene) commonly used in the food industry, therefore, the compound can be used for preparing the antioxidant or a free-radical scavenger and has wide application prospect. The 2-(2- hydroxyl-5-(methoxycarbonyl) phenoxyl) benzoic acid as well as the preparation method and the application thereof have important significance on promoting the deep processing and utilization of litchi, improving the value added of a litchi product and promoting the sustainable development of the industry. The formula (I) is shown in the specification.
US20120070467 Ophthalmic Drug Delivery The present invention includes and provides a method of delivering a medicament to an eye of a subject in need thereof a solution, the method comprising: (a) providing droplets containing the medicament with a specified average size and average initial ejecting velocity; and (b) delivering the medicament to the eye, where the droplets deliver a percentage of the ejected mass of the droplets to the eye.
WO2006047354A1 Pyrrolo [1,2-d][1,2-4]triazine as inhibitors of c-jun n terminal kinases (jnk) and p-38 kinases A compound of formula (I): wherein the substituents are as defined in the specification as inhibitor of C-Jun N terminal Kinases (JNK) and P-38 Kinases.
US20130028967 Therapeutic agent for pulmonary fibrosis Disclosed are: a substance transfer carrier to an extracellular matrix-producing cell in the lung, which comprises a retinoid; a therapeutic agent for pulmonary fibrosis, which utilized the carrier; and a preparation kit of the therapeutic agent.
CN101797328B Production process of Zhenqi capsule and test method thereof The invention belongs to a Chinese patent medicine production process and a test method thereof, in particular to a production process of a Zhenqi capsule and a test method thereof. The production process of Zhenqi capsule comprises the following five steps of 1) preparation of material, 2) processing, 3) grinding, 4) mixing and 5) granulation. The test method comprises the following five steps of a distinguishing, b. examination, c. preparation of reference product solution, d. preparation of solution to be tested and e. determination. The production process and the test method can improve the drug effect, ensures the quality and the curative effect of the medicine, and can precisely determine the quality of the product.
WO2009109679A1 Use of virgin olive oil polyphenolic compounds in cancer treatment The invention relates to the use of polyphenol compounds present in extra virgin olive oil for the treatment of cancer, as well as to pharmaceutical compositions containing same and to the use thereof in the production of drugs.
CN103083232A Edaravone injection without antioxidant and preparation method thereof The invention belongs to the field of medicine preparation, and particularly relates to edaravone injection without an antioxidant and a preparation method thereof. The invention aims at providing the edaravone injection which contains few impurities, is short in preparation time and is free of addition of the antioxidant. The edaravone injection comprises edaravone, a pH value conditioning agent and water for injection; and the preparation method comprises the steps of: A. preparing liquid; B filtering; C. filling; and D. sterilizing, wherein nitrogen is fed for protection in the previous three steps, and the remaining oxygen in the water and the impurity content of the product are strictly controlled so as to ensure the safety and effectiveness of the edaravone injection in clinical application.
US20080221060 Therapeutic Compounds Use of compounds of general formula (A) as medicaments is described, in particular for the treatment of pain or inflammation; wherein: (I) when X=OH, R2=NH2, R5=CH2OH, R6=H, R1 is C5-C6 alkoxy, OCH2Cyclopropyl, O-(2,2,3,3-tetrafluoro-cycloButyl), phenoxy, substituted phenoxy, OCH2CH2OH, or OCH2CHF2, (5-indanyl)oxy, C1, C2, C5, or C6 alkylamino, (R) or (S)-sec-Butylamino, C5 or C6 cycloalkylamino, exo-norbornane amino, (N-methyl, N-isoamylamino), phenylamino, phenylamino with either methoxy or fluoro substituents, a C2 sulfone group, a C2 alkyl group, a cyano group, a CONH2 group, or 3,5-dimethylphenyl; or when X=H, R2=NH2, R5=CH2OH, R6=H, R1 is n-hexyloxy; or (II) when X=OH, R1=H, R5=CH2OH, R6=H, R2 is NMe2, N-(2-isopentenyl), piperazinyl, (N-Me, N-benzyl), (N-Me, N—CH2Ph(3-Br)), (N-Me, N—CH2Ph(3-CF3)), or (N-Me, N-(2-methoxyethyl)), or OCH2Cyclopentyl; or (III) when X=OH, R5=CONHR3, R6=H: R1 is H, R3 is an isopropyl group, and R2 is either NH2 or a methylamino group (NHMe) or an isoamyl group (CH2CH2CHMe2); or R1 is H, R3 is H, and R2 is NH2; or R1 is OMe, R3 is Ph, and R2 is NH2; or R1 is NHCH2CH2CH2CH2CH2Me, R3 is CH2CH2CH2Me, and R2 is NH2; or (IV) when X=OH, R1=H, R2=NH2, R5=CH2NHCOR4, R6=H, R1 is n-propyl or NHCH2CH3; or (V) when X=OH, R5=CH2OH, R6=H: R1 is NHCyclohexyl when R2 is NMe2; or R1 is OMe when R2 is NHBenzyl; or (VI) when X=OH, R2=NH2, R5=CH2OH, R6=Me, R1 is NHCyclohexyl or NHCyclopentyl.
CN103554025A 3-pyrazole carboxylic acid amide compound and preparation method thereof as well as application of compound in preparation of medicaments as CB1 receptor inhibitors The invention relates to a 3-pyrazole carboxylic acid amide compound and a preparation method thereof as well as an application of the compound in preparation of medicaments as CB1 receptor inhibitors and belongs to the technical field of pharmaceutical chemistry. The general formula of the chemical structure of the compound is as shown in a formula (I), wherein R1 is 1, 5-bis-substituted phenyl-4-R9-pyrazol-3-yl, the general formula of the chemical structure is as shown in a formula (II), and the technical key points are as follows: R3 in the general formula (I) corresponds to substituting groups except amino and carboxyl in various alpha-amino acid molecules; R6 and R7 are H simultaneously or O jointly. The compound provided by the invention has in vitro activity which is equivalent to that of rimonabant, but the toxicity is obviously reduced in comparison with the rimonabant.
CN101579466A Medicine composition for reducing blood sugar and blood fat, and curing diabetes The invention relates to a medicine composition for reducing blood sugar and blood fat, and curing diabetes, comprising yam, coptis root, vitamin A, beta-renieratene, vitamin B complex, vitamin C, vitamin D, vitamin E, major elements of calcium and magnesium and trace elements of zinc, selenium, chromium, copper, molybdenum, iodine and manganese. The composition is mainly suitable for hyperglycemia, hyperlipemia and diabetes crowds, is curative for reducing blood sugar, blood fat and curing diabetes, and can be used for a long time or according to the course of treatment.
US20100076088 Crystalline form IV of agomelatine, a process for its preparation and pharmaceutical compositions containing it Crystalline form IV of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.
US20100048643 Novel Polymorph Forms Of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine Polymorph forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine p-hydroxybenzoate, and methods for their preparation, pharmaceutical composition containing said polymorph(s) and use, are disclosed. The polymorphs can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
WO2006036055A2 Method of female contraception and kit for use in such method The invention is concerned with a method of contraception in a female mammal of childbearing capability, said method consisting of two alternating phases - a preservation phase and a shedding phase - and comprising at least two sequences of (-a). a preservation phase of 3 -12 months comprising continuous oral administration to the female of dosage units containing: (i) an estrogen selected from the group consisting of 17β-estradiol, esters of 17β -estradiol and combinations thereof, in an amount equivalent to a daily oral dosage of 2.2-5 mg 17β -estradiol, and (ii) a progestogen in an amount equivalent to a daily oral dosage of 30-750 µg levonorgestrel; and (b). a shedding phase of 4-12 days during which no progestogen is administered. The invention also relates to a contraceptive kit comprising one or more packaging units comprising separately packaged, individually removable oral dosage units for use in the aforementioned contraceptive method.
WO2011043381A1 Pyrazolothiazole compound A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which has an excellent antagonistic activity on a CRF receptor. [In the formula, X represents a nitrogen atom or CH; R1 represents -A11-A12; A11 represents a single bond or an alkylene group; A12 represents a hydrogen atom, an alkyl group or a cycloalkyl group; R2 represents -A21-A22; A21 represents a single bond or an alkylene group; A22 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a non-aromatic heterocyclic group, a heteroaryl group or the like; R3 represents an alkyl group, a cycloalkyl group, an alkoxy group, a cycloalkoxyalkyl group, a dialkylamino group, a halogen atom, a cyano group, a formyl group, a carboxyl group or the like; R4 represents a hydrogen atom or an alkoxy group; R5 represents a halogen atom, an alkyl group or an alkoxy group; R6 represents a hydrogen atom, an alkyl group, an alkoxy group, an alkylthio group, an alkylsulfinyl group or the like; and R7 represents an alkyl group, an alkoxy group or an alkylthio group.]
EP1037632B1 Benzothiazole protein tyrosine kinase inhibitors Novel benzothiazoles and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.
CN101723926A Isoflavone derivative and preparation method and application thereof The invention relates to an isoflavone derivative and a preparation method and application thereof, which belong to the field of chemical medicaments. The technical problem solved by the invention is to provide the isoflavone derivative and the preparation and the application thereof. The isoflavone derivative has a structural formula as shown by (I), wherein R1 and R2 in the structural formula are C1-C5 alkyls. The isoflavone derivative has a significant effect of resisting Coxsackie viruses, can be used for preparing medicaments for resisting the Coxsackie viruses, and has an intensive application prospect.
US20110046067 COMPOSITIONS COMPRISING HUMAN EGFR-siRNA AND METHODS OF USE The present invention provides nucleic acid molecules that inhibit EGFR expression. Methods of using the nucleic acid molecules are also provided.
CN103251558A Preparation of high drug loading multifunction nanometer drug with combination treatment effect The invention discloses preparation of a high drug loading multifunction nanometer drug with a combination treatment effect, wherein an oversaturation degree of a hydrophobic anti-cancer drug in water, a cation type surfactant concentration, and the amount of an added Au seed are controlled, and a chemical effect between a disulfide bond in a hydrophilic surfactant and the surface of a Au shell is adopted to carry out hydrophilic modification on the surface of a nanometer drug so as to achieve preparation of high drug loading multifunction nanometer drug with characteristics of chemotherapy and thermotherapy combination treatment effect and stable bioenvironment, wherein a layer of a Au shell grows on the nanometer drug. With the technical scheme, the preparation method is simple, experimental basis is provided for preparation of other multifunction nanometer materials for cancer treatments, and wide applications can be provided for the fields of biology, medicine, chemistry and the like.
US20100331304 Compounds Which Modulate The CB2 Receptor Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
WO2007060899A1 Application of actin-binding protein to disease associated with cell motility It is intended to identify a protein involved in a molecular mechanism between Akt and cell motility as well as to elucidate its function and to find its application. In the invention, for achieving the above object, by using a protein containing an amino acid sequence identical or substantially identical to the amino acid sequence represented by SEQ ID NO: 2 or a partial peptide thereof, a compound that activates or inhibits any of cell motility, cell migration and angiogenesis or a salt thereof is screened.
CN103007286A Solid medicine composition of tolvaptan The invention discloses a solid medicine composition of tolvaptan. The solid medicine composition of tolvaptan comprises granular or unformed powder of tolvaptan, sugar and a sugar alcohol diluent. The preparation method comprises the following steps of: highly dispersing the active component tolvaptan into the diluent to obtain solid dispersoid; and preparing into oral solid preparation with pharmaceutically acceptable auxiliary materials. The solid medicine composition is clinically used for treating hyponatremia.
CN103006797A Throat heat clearing tablet and preparation method The invention discloses a throat heat clearing tablet and a preparation method of the tablet. The method comprises the following steps of; (1) taking indigo naturalis, liquorice, fructus chebulae, menthol, borneol and calculus bovis factitious; (2) carrying out water-extracting on the fructus chebulae, filtering the extracting solution, condensing the filtered extracting solution to obtain an extract 1, subjecting the extract 1 to ethanol precipitation, and recycling the ethanol to obtain the fructus chebulae extract, adding aqueous solution of hydrochloric acid into the indigo naturalis for soaking, washing the soaked indigo naturalis to be neutral, and drying the washed indigo naturalis to obtain the refined indigo naturalis, adding water into the liquorice for extracting, filtering the extracting solution, condensing the filtered extracting solution to obtain an extract 2, adding ethanol into the extract 2, settling the resulting solution, taking supernatant from the settled solution, adjusting the pH value of the supernatant, filtering the pH-adjusted supernatant, recycling the ethanol from the filtrate, adding water into the ethanol-free solution, adjusting the pH value of the resulting solution, filtering the pH-adjusted solution, washing the sediment, and drying the washed sediment to obtain the liquorice extract, and (3) drying and crushing the fructus chebulae extract, mixing the crushed fructus chebulae extract with the crushed refined indigo naturalis, calculus bovis factitious, borneol, menthol, and liquorice extract uniformly to obtain a mixture, adding a lubricant and a diluent into the mixture to mix uniformly, and tabletting the resulting mixture. The throat heat clearing tablet provided by the invention is low in cost, safe, fast in taking effect, good in curative effect, and convenient to carry about. The preparation of the tablet takes little working hours, transfer rates of effective components are high, and the safety of an operator is ensured.
US20080289057 Sperm factor sequences A nucleic acid sequence, including an isolated, purified or recombinant nucleic acid sequence, includes: (a) a nucleic acid sequence encoding a polypeptide encompassed by the present invention, namely, a PLC-zeta; PLCζ amino acid sequence, capable of triggering calcium oscillations in oocytes; (b) a sequence substantially homologous to or that hybridizes to sequence (a) under stringent conditions; (c) a sequence substantially homologous to or that hybridizes to the sequences (a) or (b) but for degeneracy of the genetic code; and (d) an oligonucleotide specific for any of the sequences (a), (b) or (c) above.
WO2008084240A1 Chemical compounds 636 : pyridopyrimidinediones as pde4 inhibitors The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE 4 mediated disease state.
CN102961328A Levofloxacin injection and preparation method thereof The invention relates to a levofloxacin injection. The levofloxacin injection is characterized in that the injection is a faint yellow solution, the pH value of the injection is 6.0-7.5, and the injection comprises the following ingredients in parts by weight: 10-20 parts of levofloxacin, and 0.1-0.3 part of chelating agent. The preparation method comprises the steps: firstly, mixing and dissolving levofloxacin and sodium hydroxide into water, then adding the chelating agent, and finally adding one or two of lactic acid and butyrate, so as to enable the solution to form a faint yellow transparent solution which is stable in property and has no crystallization separation after being stored for a long time. The transparent solution is faintly acidy, and suitable for biological environment in livestock and poultry organisms, is non-irrtant, and livestock and poultry can not be maladaptive, the levofloxacin effective component is high in content and can be directly absorbed by the livestock and poultry organisms, and the single-time administration treatment effect is good.
CN1948306A Fluoroquinolone-oxazolidone derivative, its preparation method and application The present invention discloses a new-type fluoroquinolone-oxazolidone derivative, its preparation method and application. Said derivative has good antibacterial action. Besides, said invention also provides its structure general formula.
CN103040744A Propyl gallate liposome injection The invention discloses propyl gallate liposome injection and a preparation method thereof. The propyl gallate liposome injection with excellent quality is prepared by selecting propyl gallate, dilauroyl phosphatidyl glycerol, cholesterol, tween 80, sodium hydrogen sulfite, ethylene diamine tetraacetic acid (EDTA)-2Na and dextranum. Compared with the conventional preparation, the preparation provided by the invention has the advantages that the stability and the bioavailability of the preparation is greatly improved, the medicine release is stable, the quality of the preparation product is improved, the toxic or side effect is reduced and obvious curative effect is achieved.
CN102198088B Cervical slow-release suppository for treatment of cervical erosion and preparation method thereof The invention discloses a cervical slow-release suppository for the treatment of cervical erosion and a preparation method thereof. The cervical slow-release suppository comprises a columnar cervical canal body with one end being a plane and the other end being a curved surface body protruding outwards in the axial direction, the cervical canal body and the curved surface body are structurally integrated to form a medicine-containing body, the circumferential diameter of the curved surface body is larger than the outer diameter of the cervical canal body, the middle parts of the cervical canal body and the curved surface body are provided with through holes, the inner wall of each through hole is provided with an isolating layer, and the cervical canal body and the curved surface body areprepared from the raw materials in the weight ratio: 100-200g of matrine, 100-200g of oil of zedoary turmeric, 50-75g of borneol, 60-90g of chitosan, 50-90g of sodium hyaluronate, 70-100g of polyethylene glycol, 50-70g of lactic acid oligomer and 200-300g of lactic acid-hydroxyacetic acid-Epsilon-caprolactone copolymer; the cervical slow release suppository can be directly delivered into cervicalcanal and the effective ingredients of the suppository can be continuously released for 20 days, therefore, direct administration to the affected parts is realized.
WO2014161801A1 Piperazino[1,2-a]indol-1-ones and [1,4]diazepino[1,2-a]indol-1-one The present invention relates to compounds of general formula I wherein R1 is halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or cyano; R2 is hydrogen, CF3 or lower alkyl; R3 is hydrogen, lower alkyl, lower alkenyl, lower alkinyl, heterocycloalkyl, lower alkyl substitueted by cyano, cyano, benzyl substituted by halogen, 2-oxa-6-aza-spiro[3.3]hept-6-yl or is lower alkoxy substituted by halogen; X is -CH2- or -CH2-CH2-; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
WO2013066368A1 Use of mirna 126 to produce hematopoietic stem cells What is described is a method for modulating the phenotype of a stem progenitor cell (SPC), including hematopoietic SPC (HSPC), comprising contacting the stem-progenitor cell with one or more nucleic acid molecules, in which each of the nucleic acid molecules comprises a nucleotide sequence that is at least about 90% identical to a sequence of miR126 (e.g., SEQ ID NOs: 1 or 2), or the complements thereof. Upon such contact, expression VCAM-1 is inhibited, resulting in mobilization of SPC. The miR126 nucleic acids may be administered to a healthy subject, and blood cells may be collected from the subject and used for allogeneic transplantation with greater ease than current procedures.
DE102009015917A1 Use of an active agent comprising resveratrol, thymol, xanthohumol or vitamin C for inhibition and/or prophylaxis of e.g. eryptosis, acute renal failure, anemia, shock, atherosclerosis, thrombosis, diabetes mellitus and sickle cell anemia Use of an active agent (I) comprising resveratrol, thymol, xanthohumol or vitamin C or its derivatives and/or salts for preparing an agent for inhibition and/or prophylaxis of eryptosis, is claimed. - ACTIVITY : Anabolic; Antibacterial; Immunosuppressive; Nephrotropic; Antianemic; Vasotropic; Antiarteriosclerotic; Anticoagulant; Antidiabetic; Hemostatic; Antiarthritic; Antirheumatic; Metabolic; Antisickling; Antiapototic. - MECHANISM OF ACTION : None given.
CN103739578A Zinc ascorbate hydrogen citrate, as well as preparation method and application thereof The invention relates to a new substance, namely zinc ascorbate hydrogen citrate, as well as a preparation method and an application thereof. The preparation method of the zinc ascorbate hydrogen citrate is characterized by comprising the following steps: (1) weighing raw materials, namely citric acid monohydrate, ascorbic acid, zinc oxide and water, and putting into a reaction kettle, wherein the weight ratio of the substances, namely the citric acid monohydrate, the ascorbic acid and the zinc oxide is 3: 1: 4; (2) starting a machine for performing chemical reaction for half an hour; (3) stopping the machine for half an hour, adding ethanol and enabling the chemical reaction to be mature; and (4) starting the machine for half an hour, and releasing the zinc ascorbate hydrogen citrate. The zinc ascorbate hydrogen citrate prepared by the preparation method provided by the invention can be dissolved in water, be conductive to absorption by people and animals, and be used as a zinc supplement Vc anti-oxidation preservative, a zinc supplement Vc food additive or medicines for treating bad appetite, dysplasia, stomach diseases, bronchitis, asthma, pneumonia, hepatitis, liver cancer and hypertension.
US20110076345 Herbal Formulation for the Treatment of Bone Fractures and Osseous Defects An herbal formulation including Symphytum Officinalis extract and Phytolacca Decandra extract may be combined to treat bone fractures and osseum defects. Specifically, the herbal formulation provides for the regeneration of osseum tissue for treating bone defects such as imperfect osteogenesis, pseudo-arthrosis infected or not, bone union delay of fractures, osteoporosis, osseum tumors, aneurismatic osseum cyst, and myeloma multiple.
US20110224187 Pyrrolidine, piperidine and piperazine derivatives and methods of use thereof The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
WO2014090174A1 Nanoscale capecitabine and preparation method therefor A nanoscale capecitabine particle and a preparation method therefor. The particle uses silica aerogel as a carrier. Capecitabine is adsorbed in pores of the silica aerogel, forming the capecitabine particle having a diameter of 100 nm or less. The silica aerogel has a porosity of 95-99%, an aperture of 10-50 nm, a specific surface area of 200-1000 m2/g, and a density of 3-300 kg/m3, and the diameters of gel particles forming a network are 1-50 nm.
WO2006005856A1 Use of polyphenol ethylene organometallic derivatives for treating a non-hormone dependent cancer The invention concerns polyphenol ethylene organometallic derivatives of formula (I) for preparing a medicine for preventing and/or treating a non-hormone-dependent cancer. The invention concerns novel polyphenol ethylene organometallic derivatives of formula (I), wherein either (i) one of R1 and R2 represents a group (A) and the other represents an organometallic group, or (ii) R2 represents a group (A) and R1 and R3 together with C=C form an organometallic group, or (iii) R2 represents a group (A) and -YR3C=CR1-forms an organometallic group, R'1, R'2, R'3, R''1, R''2, R''3, identical or different represent a group selected among a hydrogen atom, a hydroxyl group, a C1-C6 alkyl group, a halogen atom, a C1-C6 halogenoalkyl group, a -OCOR4 group, wherein R4 represents a C1-C16 alkyl group, a C1-C16 halogenoalkyl group or an aryl group.
CN101607942A Novel imidazolone anti-tumor compound and preparation method thereof The invention relates to the technical field of medicaments, in particular a compound capable of inhibiting the growth of tumor cells. The compound has a structural general formula on the right, wherein X can be -NH- or -O-. The R radical is various substituted benzene rings, naphthalene rings and indole rings. The substituting positions of the radicals on an aromatic ring are not limited, which can be 2 sites, 3 sites and 4 sites. The substitution can be mono-substitution and poly-substitution (including di-substitution, tri-substitution or tetra-substitution), and substituents in the poly-substitution can also be interconnected into rings. The substituents in the benzene rings comprise: (1) H, F, Cl, Br and I; (2) low grade alkyl groups such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl and tert-butyl; (3) low grade alkoxy groups such as methoxyl and oxethyl; and (4) hydrogen bond receptors and donor radicals such as cyano-groups, nitro-groups, amino-groups and hydroxyl. The compound has stable chemical properties, can inhibit the growth of the tumor cells, and can be applied to preparing anti-tumor medicaments.
WO2011150229A3 Dietary supplements containing extracts of cinnamon and methods of using same to promote enhanced sirtuin, cell and telomere integrity A dietary supplement composition is provided for enhancing the expression of a sirtuin gene or protein. An inventive supplement composition includes at least one cinnamon extract containing at least 0.5% doubly linked Type-A polymers by dry weight. The cinnamon extract is derived from the Cinnamonum aromaticum, Cinnamonum verum or Cinnamonum burmannii plant. In some embodiments, the cinnamon extract is present at approximately 20%-50% of the dry weight of the composition. A vitamin, weight loss agent, or antioxidant is optionally provided in the composition. The dietary supplement composition is administered orally to promote expression or enhanced expression of a sirtuin gene or protein.
CN101642434B Levofloxacin lactate liposome sodium chloride injection and preparation method thereof The invention provides a levofloxacin lactate liposome sodium chloride injection and a preparation method thereof. The levofloxacin lactate liposome sodium chloride injection is characterized by being prepared with the following components according to parts by weight: 1 part of levofloxacin lactate, 5-15 parts of phospholipid, 0.5-1.5 parts of cholesterol, 0.5-2 parts of deoxycholate, 2-10 partsof sodium chloride and 0.5-1.5 parts of antioxidant. The invention adopts specific auxiliary materials to proportion with the original auxiliary materials and adopts the reverse phase evaporation method to prepare the levofloxacin lactate liposome sodium chloride injection of the invention, solving problems of unqualified levofloxacin lactate injection clarity and insoluble particles, and yellowing of solution color in the prior art. The invention provides a stable levofloxacin lactate liposome sodium chloride injection featuring long-time laying aside.
WO2013088084A1 Phytoecdysones for use in improving the muscle quality of obese and/or sarcopenic mammals The invention relates to phytoecdysones for use in improving muscle quality in obese and/or sarcopenic mammals. More particularly, the invention relates to the obese mammals subjected to a low‑calorie diet. The phytoecdysones are advantageously incorporated into a food composition. According to the invention, the phytoecdysones can be derived from plants, such as quinoa.
US20120003270 6-substituted isoflavonoid compounds and uses thereof The present invention relates to 6-substituted isoflavonoid compounds and compositions comprising same. The invention further relates to the use of 6-substituted isoflavonoid compounds for the treatment of various diseases and conditions.
CN102357263A Composite inducer for promoting autologous peripheral preadipocyte proliferation and enlargement for cosmesis and body beautification and preparation method thereof The invention provides a composite inducer for promoting autologous peripheral preadipocyte proliferation and enlargement for cosmesis and body beautification and a preparation method thereof. The invention adopts an inducer system for promoting autologous peripheral preadipocyte proliferation and differentiation which comprises three liquid-phase water-soluble, or oil-soluble, or alcohol-soluble functional components, allows preadipocytes to perform limited proliferation and ordered differentiation by in-vitro cell culture or in a manner of in-vivo induction and stimulation, realizes and achieves the increase of subcutaneous adipocyte quantity and volume, maintains the cell blood supply and nutrition, keeps and maintains the normal survival, growth and life activity of adipocytes under physiological conditions, results in the increase of the adipocyte quantity and the increase of the cell volume, and reaches obvious and natural breast plumping effect; the main components of the inducer of the invention come from autologous tissues and natural plant components, and the system is applied to a local part, and has high safety; in addition, the system is simple in preparation, is economical, and has wide market prospects.
US20110008304 Use of cells to facilitate targeted delivery of nanoparticle therapies The present invention is related to the use of cells, such as stem cells or immune system cells, to deliver nanogels comprising an active agent to a desired site in the body. The present invention utilizes cells as a delivery system for active agents that are difficult to deliver, such as active agents with poor solubility, that degrade easily, or that are toxic to the body. The nanogels are preferably non-toxic and can optionally include a lytic agent to program apoptosis of the cell to deliver the nanogel and active agent to a desired sire within the body.
US20120071538 Pharmaceutical formulatons Good bioavailability of desmopressin can be obtained by means of an orodispersible pharmaceutical dosage form. Preferred dosage forms comprise desmopressin and an open matrix network which is an inert water-soluble or water-dispersible carrier material. Desmopressin formulated in this way is useful for voiding postponement, or the treatment or prevention of incontinence, primary noctural enuresis (PNE), nocturia or central diabetes insipidus. Peptides other than desmopressin can also be formulated in this way.
US20110135713 Antimicrobial and Antiviral Compounds and Methods for Their Use The present invention provides protonated compounds having antiviral and antimicrobial activity. The invention also provides antimicrobial compositions comprising protonated compounds of the invention. The protonated compounds of the invention provide efficacious antimicrobial activity against resistant strains of bacteria and opportunistic fungi. The invention also provides antiviral compositions comprising compounds of the invention. Viruses that may be treated by compositions of the invention include, but are not limited to, HIV, HSV, CMV, HBV, HCV and influenza virus.
WO2011131741A1 Heterocyclic carboxylic acid amides as pdk1 inihibitors The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
US20050245537 Use of compounds having ccr antagonism It is intended to provide preventives/remedies for graft-versus-host disease and/or rejection in organ or bone marrow transplantation, rheumatoid arthritis, autoimmune diseases, allergic diseases, ischemic cerebral cell injury, myocardial infarction, chronic nephritis and arteriosclerosis. The above object can be achieved by preventives/remedies for graft-versus-host disease and/or rejection in organ or bone marrow transplantation, rheumatoid arthritis, autoimmune diseases, allergic diseases, ischemic cerebral cell injury, myocardial infarction, chronic nephritis and arteriosclerosis characterized by containing a specific compound having a CCR (CC chemokine receptor) antagonism.
US20090317492 Therapeutic Composition and Use The use of liquid formulations in the preparation of a medicament for the prevention and treatment of oral, gastric and digestive infections and in particular for the prevention of ventilator associated pneumonia as well as liquid enteral and parenteral tube feeding compositions. The feeding compositions are suitable for use in the prevention of ventilator associated pneumonia.
CN102836153A Compound buccal tablet The invention discloses a compound buccal tablet, which is prepared by adding medicinal adjuvants into daphnoretin and andrographolide as active ingredients, wherein the weight ratio of daphnoretin to andrographolide is 1 to (0.5-8). The buccal tablet can directly reach up to the focuses when the relevant diseases in a throat part are treated, the buccal tablet can be placed at the hypogloeeis or between the gum and the cheek so as to be absorbed through the mouth mucosa or the hypoglossal mucosa, so that the first-pass effect caused by the liver can be effectively avoided when the buccal tablet is taken, and the bioavailability of the buccal tablet can be greatly improved.
EP2641592A1 Pharmaceutical formulation comprising bendamustine The present invention is related to the field of pharmaceutical compositions for the treatment of various disease states, particularly neoplastic diseases and autoimmune diseases. It especially relates to the oral application of bendamustine and its derivatives. The invention further relates to a process for preparing a pharmaceutical composition which comprises bendamustine and its derivatives prepared by hot melt extrusion using pharmaceutically acceptable excipients. The invention also relates to such pharmaceutical compositions and hot melt extrudates.
WO2012098692A1 Composition for inhibiting target gene expression Provided is a composition or the like containing lipid particles packed with double-stranded nucleic acid molecules, the composition being a polynucleotide 17 to 30 nucleotides long which has an antisense strand comprising a nucleotide sequence complementary to a consecutive 17-nucleotide sequence of a target gene mRNA, and which has a sense strand comprising a nucleotide sequence complementary to the 1st to 17th nucleotide toward the 3' terminus from the 5' terminus of the antisense strand, where saccharides for binding to a nucleotide at a specific location of the antisense strand and the sense strand are, each at a specific ratio, a deoxyribose, or a ribose in which the hydroxyl group at position 2' has been substituted with a modifying group. The lipid particles are lipid particles having a lipid bilayer membrane, a constituent component of which is a lipid derivative of a water-soluble substance, a fatty acid derivative, or a derivative of an aliphatic hydrocarbon.
CN101016264A Nitroimidazole derivative for treatment, preparing method and use The invention discloses a manufacturing method and applying method of nitro imidazole derivant, which is fit for human and other mammal infected by anaerobe and parasite.
US20130095089 Glucosylceramide synthase inhibitors and therapeutic methods using the same Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
CN101416970A Use of arjunolic acid in preparing glycosidase inhibitor The invention provides the application of arjunolic acid or salts thereof suitable for medical purpose in the preparation of a drug of an Alpha-glucosidase inhibitor. The invention is characterized in that strong effective Alpha-glucosidase inhibitor is extracted and separated from lagerstroemia plants which has rich source, are easy to be extracted and can be recycled for a plurality of times, thus not only promoting economic benefit, but also being environment-friendly. Furthermore, the monomeric compound product of the Alpha-glucosidase inhibitor is stable and is convenient to be stored. Pharmacological tests prove that the arjunolic acid has powerful effect in inhibiting Alpha-glucosidase, wherein, physiological change or diseases caused by or related to the Alpha-glucosidase includes but is not limited to Type II Diabetes. The monomeric compound product of the Alpha-glucosidase inhibitor can be further developed into the drugs for clinically treating NIDDM, thereby having better prospect for marketization. The constitutional formula of compound of the arjunolic acid is shown as above.
US20050164278 Breast cancer specific genes (BSG) and diagnosing/preventing cell proliferative disorders; immunotherapy; paramagnetic imaging The invention relates to BSG polypeptides, polynucleotides encoding the polypeptides, methods for producing the polypeptides, in particular by expressing the polynucleotides, and agonists and antagonists of the polypeptides. The invention further relates to methods for utilizing such polynucleotides, polypeptides, agonists and antagonists for applications, which relate, in part, to research, diagnostic and clinical arts.
CN103467477A Procyanidin A2, and preparation method and application thereof The invention discloses procyanidin A2 and a preparation method and application thereof. Procyanidin A2 has a structural formula as represented by formula (I). According to the invention, a procyanidin compound--procyanidin A2 is prepared and separated from litchi liquid, and yield of procyanidin A2 is as high as 1.26 to 5.26 g/kg (while purity is 80 to 90%); results of activity experiments show that the compound has good antioxidant activity which is substantially better than that of a synthesized anti-oxidant BHT frequently used in the food industry and the compound can be used for preparation of an anti-oxidant or free-radical scavenger; moreover, the compound has good antineoplastic activity, can effectively inhibit propagation of human liver cancer Hep-G2 cells and human cervical carcinoma Hela cells, is used for preparation of antitumor drugs and has wide application prospects. The invention is of critical significance to promotion of deep processing of litchi, increase of added values of litchi products and promotion of sustainable development of the processing industry of litchi.
EP1169032B1 Ketoprofen microgranules, method for preparing the same and pharmaceutical compositions The invention concerns ketoprofen microgranules with prolonged release each consisting of an active core containing ketoprofen coated with a polymeric film enabling prolonged release of the active principle and containing Eudragit DOLLAR mR(3) RL and Eudragit 3 Rs in a volume proportion substantially equal to 90/10.
EP2026788B1 Therapeutic combination for painful medical conditions A therapeutic combination comprises a first agent comprising a compound as defined herein, illustratively lacosamide, or a pharmaceutically acceptable salt thereof, and a second agent effective in combination therewith to provide enhanced treatment of pain associated with or caused by a medical condition, by comparison with the first agent alone. The combination can be provided in a single dosage form or separate dosage forms and is illustratively useful for treatment of an arthritic condition and/or pain related thereto.
US20090182021 Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease The present invention is directed to tricyclic compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
US6943194 oxidizing 3-(tert-butyl dimethylsilyl)oxy-4-methoxybenzaldehyde with potassium permanganate to form carboxylic acid, converting to corresponding acid chloride, protecting with a butyllithium derivative, deprotecting to form phenstatin A newly discovered antineoplastic compound denominated “phenstatin” is herein described as are synthetic methods for producing phenstatin and the active prodrug thereof. Phenstatin was converted to the sodium phosphate prodrug (3d) by a dibenzylphosphite phosphorylation and subsequent hydrogenolysis sequence 3b→3c→3d. Phenstatin (3b) was found to be a potent inhibitor of tubulin polymerization and the binding of colchicine to tubulin comparable to combretastatin A-4 (1b).
CN1985831A Lung-targeting cefradine microsphere for animal and birds and its preparing method The present invention belongs to the field of veterinary medicine technology, and is especially lung targeting cefradine microsphere for animal and its preparation process. The cefradine microsphere is prepared with cefradine as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving cefradine in gelatin solution and adding Span-80 and liquid paraffin through stirring to obtain emulsion; cooling in icy bath to below 5 deg.c and adding glutaraldehyde through stirring for cross-linking and curing; dewatering with isopropyl alcohol and suction filtering; washing with isopropyl alcohol and ethyl ether to eliminate glutaraldehyd, washing with petroleum ether to eliminate liquid paraffin in the surface of microsphere and vacuum drying at room temperature to obtain cefradine microsphere. The medicine has raised tissue selectivity, delayed release, raised curative effect and lowered toxic side effect.
US20080193425 Methods for administering fgf18 FGF18 is known to stimulate the proliferation of chondrocytes, resulting in increased cartilage formation. When hyaluronic acid is administered in addition to FGF18, the effects on chondrocyte proliferation and production of matrix were found to be greater than administration of FGF18 or hyaluronic acid alone.
WO2014030688A1 Chromone derivative having linear side chain The purpose of the present invention is to provide a compound having bone formation promoting activity. The solution is a compound having general formula (I) or a pharmaceutically acceptable salt thereof. [In the formula, R1 is a methyl group, etc., R2 is a hydroxyl group, etc., R3 is a hydrogen atom, etc., R4 is a methyl group, etc., and A is a hydrogen atom, etc.]
EP2724724A1 Treatment and prevention of epithelial infections with copper and zinc chelates Provided herein are sprayable copper and zinc chelate formulations for the treatment and prevention of epithelial infections in sheep, goats, horses, and cattle. More particularly, the compositions comprise micronized copper and zinc chelates suspended in a liquid, wherein the total amount of copper and zinc chelate ranges from 5 to 50 percent by weight; and less than 5% (w/v) of the chelates are dissolved.
CN101982170A Amide compound and application thereof in preparing monoamine oxidase inhibitor The invention provides a new amide compound shown as structural formula (I) and application thereof in preparing monoamine oxidase inhibitor. The invention takes phenols compound shown as formula (II) and 2-chloroacetamide shown as formula (III) as reaction substrate, reaction is taken place to obtain amide compound shown as the formula (I), and then fluorescence detection method is used for detecting monoamine oxidase inhibition activity. The method has simple operation process, raw materials are available, and the obtained monoamine oxidase inhibitor has stable properties, and purity is high (more than 99%); compared with the previously researched method of monoamine oxidase inhibitor, the sieved novel amide monoamine oxidase inhibitor has simple structure, and inhibition activity and selectivity on MAO-A and MAO-B are all greatly improved.
WO2011151618A3 Compounds for the treatment of clostridium difficile associated disease (cdad) Disclosed are compounds of formula (I): or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.
WO2011109470A1 Heteroaryl nitrile compounds useful as inhibitors of cathepsin-s Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.
US20100240620 3-Cyano-5-thiazaheteroaryl-dihydropyridine and the use thereof for the treatment of cardiovascular diseases The present application relates to novel aryl-substituted 3-cyano-5-thiazolyl- and 3-cyano-5-thiadiazolyl-1,4-dihydropyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
CN102432639A 1-(2-hydroxy-3-(phenylamino)propyl)-3-ferrocenyl-1H-pyrazole-5-ethyl formate compound and medicinal use thereof The invention discloses a 1-(2-hydroxy-3-(phenylamino)propyl)-3-ferrocenyl-1H-pyrazole-5-ethyl formate compound and a medicinal use thereof. The 1-(2-hydroxy-3-(phenylamino)propyl)-3-ferrocenyl-1H-pyrazole-5-ethyl formate compound is a chiral 1-(2-hydroxy-3-(phenylamino)propyl)-3-ferrocenyl-1H-pyrazole-5-ethyl formate derivative. A result of a pharmacological experiment shows that the 1-(2-hydroxy-3-(phenylamino)propyl)-3-ferrocenyl-1H-pyrazole-5-ethyl formate compound has an obvious effect of inhibiting lung cancer cell proliferation; and lung cancer cell A549 inhibition activity of the 1-(2-hydroxy-3-(phenylamino)propyl)-3-ferrocenyl-1H-pyrazole-5-ethyl formate compound is superior to lung cancer cell H322 inhibition activity of the 1-(2-hydroxy-3-(phenylamino)propyl)-3-ferrocenyl-1H-pyrazole-5-ethyl formate compound. Therefore, the 1-(2-hydroxy-3-(phenylamino)propyl)-3-ferrocenyl-1H-pyrazole-5-ethyl formate compound as a novel ferrocenyl group-containing chiral pyrazole derivative has clinical application development prospects and has important meaning to antitumor drug development.
WO2006074223A3 Pharmaceutical compounds as activators of caspases and inducers of apoptosis and the use thereof Disclosed are 1-arylamino-phthalazines, 4-arylamino-benzo[d][1,2,3]triazines, and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
US20090258019 Diagnosis of carcinoma using RAIG1 polypeptides The present invention relates to the new uses of a polypeptide (retinoic acid-inducible gene 1; RAIG1, also known as hypothetical protein FLJ10899 or retinoic acid induced 3) compositions comprising the polypeptide, including vaccines, antibodies that are immunospecific for the polypeptide and agents which interact with or modulate the expression or activity of the polypeptide or the expression of the nucleic acid which encodes the polypeptide. The use of the polypeptide in the diagnosis, screening and treatment of carcinoma, e.g. breast cancer, pancreatic cancer, lung cancer, liver cancer, ovarian cancer, colon cancer and/or osteosarcoma, is also provided.
WO2007119624A1 Nucleoside derivative having antiherpesvirus activity Disclosed is a compound represented by the formula I below or a salt thereof. Also disclosed is a pharmaceutical composition for preventing or treating herpesvirus infectious diseases, which contains the compound represented by the formula I below or a salt thereof as an active ingredient. Formula I: [Chemical formula 23] (In the formula, R represents a hydroxy, a C1-6 alkoxy, a halogen, an NR1R2 (wherein R1 and R2 independently represent a hydrogen or a C1-3 alkyl), a cyano or a phenyl.)
WO2006009325A1 Metalloprotease inhibitor A J5 inhibitor containing a compound represented by the general formula (I): (wherein the symbols have the same meanings as in the description), a salt thereof, a solvate of either, or a prodrug of any of these. The compound having J5 inhibitory activity can be used for the prevention and/or treatment of inflammatory diseases, autoimmune diseases, allergic diseases, and skin diseases.
US20080214566 Bioavailability, solubility; free drug form; schizophrenia Provided is amorphous form of ziprasidone mesylate and process for its preparation. Also provided is a process for preparing ziprasidone mesylate dihydrate needle crystals.
CN103417526A Application of salvianolate in preparation of kidney protective agent drugs The invention provides application of salvianolate in preparation of kidney protective agent drugs. A study on effects of injection-use salvianolate on acute myocardial perfusion in acute myocardial infarction direct PCI (percutaneous coronary intervention) and prognosis founds that: subjects using the injection-use salvianolate, compared with other group subjects, after use of a contrast agent, may not have severe kidney injuries, and the injection-use salvianolate has a kidney protective effect. The invention also provides the application of magnesium lithospermate B in preparation of the kidney protective agent drugs. Effects of the magnesium lithospermate B on kidney microcirculation and overall hemorheology are studied through use of spontaneously hypertensive rats. Experiments prove that the magnesium lithospermate B in physiological and pathological states both can dose-dependently improve kidney cortex microcirculation, and show that the kidney protective effect of the magnesium lithospermate B is realized through direct improvement of the kidney microcirculation, so that the salvianolate and the magnesium lithospermate B can be used for preparation of the drugs for the prevention and treatment of the kidney injures caused by the contrast agent. The application of the salvianolate in preparation of the kidney protective agent drugs has great clinical application value.
WO2012049346A1 Hypocholesterolemic, anti-inflammatory and antiepileptic neuroprotective compound The invention relates to a compound having formula (I), the hydroxy acid thereof, the pharmaceutically acceptable salts of said hydroxy acid and prodrugs and pharmaceutically acceptable solvates of the compound and the hydroxy acid form thereof, and, in particular, the compound, the hydroxy acid form and salts thereof, etc. for use in the prevention of: neurodegenerative diseases, cognitive impairment, diseases associated with unwanted oxidation, pathological processes associated with age and progeria, cardiovascular diseases, such as atherosclerosis, auricular fibrillation, dyslipemia, hypercholesterolaemia, hyperlipidaemia and hypertriglyceridemia, inflammation or inflammatory processes, or epilepsy, epileptic seizures and convulsions.
CA2267109C Use of conjugated linoleic acid to enhance natural killer lymphocyte function A method of enhancing the activity of natural killer lymphocytes and a method for increasing the basal level of natural killer activity in an animal include the step of administering orally or parenterally to said animal a safe amount of CLA, said amount being effective to enhance the activity of killer lymphocytes or to enhance the basal activity of killer lymphocytes in the animal.
US20120289532 Method for the production of amorphous rifaximin The present invention relates to a new amorphous form of rifaximin and to methods for the preparation thereof by means of high energy milling or Spray drying. The present invention further relates to a new amorphous form for use as medicament and to the pharmaceutical compositions composing it.
CN102249945A Salicyloyl anilines compound as well as preparation method and application thereof The invention belongs to the field of medical compounds and relates to a salicyloyl anilines compound as well as a preparation method and application in preparing an anti-cancer medicine. According to the method disclosed by the invention, the salicyloyl aniline is taken as a parent and different side-chain substituent groups are introduced into a benzene ring of the parent to prepare the salicyloyl anilines compound of the following formulas, wherein in the formulas, R1, R2, R3 and R4 are defined as an specification. Compared with the Lapatinib, the prepared salicyloyl anilines compound represents that the IC50 value is obviously reduced or is at least equal to that of the Lapatinib. The experiment shows that the salicyloyl anilines compound provided by the invention has an obvious inhibition effect on tumor cells, especially ovarian cancer cells so that the salicyloyl anilines compound can be further used for preparing antitumor medicines. The chemical formula of the salicyloyl anilines compound is represented by the following formulas.
EP1562547B1 Method of stimulating hair growth using benzopyrans The present invention is directed to methods of stimulating hair growth by administering selected benzopyran compounds, to their use in the manufacture of medicaments for alopecia and to pharmaceutical compositions for alopeica, especially topical compositions.
US20110230456 Nitridoosmium(VI) Complexes for Treatment of Cancer The invention relates to nitridoosmium complexes and methods of using these compounds as treatments for cancer.
US20090226528 Encapsulated nanoparticles for nucleic acid delivery Methods and compositions for delivering agents (e.g., gene silencing agents) and molecules to cells using yeast cell wall particles are presented herein. Embodiments of the invention are particularly useful for the delivery of nucleic acids (e.g., siRNAs) to cells.
CN102988388A Application of Houttuynoid B to preparation of medicine for rising platelets The invention relates to a new application of a compound Houttuynoid B in the field of pharmacy, and particularly relates to an application of Houttuynoid B to preparation of a medicine for rising platelets, which is made public for the first time. As a framework type is brand-new, and the activity of the Houttuynoid B for treating low platelets is unexpectedly strong, the possibility of obtaining any revelation from other compounds does not exist, and the Houttuynoid B has remarkable substantive distinguishing features and obviously has a notable progress to prevention and treatment of the low platelets.
WO2009050595A3 An improved process for preparing a 2,4-thiazolidinedione derivative The present invention relates to a process for preparing rosiglitazone maleate with a low content of undesired by-products.
CN101019834A Prepn of 7-ethyl-10-hydroxycamptothecine liposome for injection The preparation process of 7-ethyl-10-hydroxycamptothecine liposome for injection includes dissolving mixture of phospholipide, cholestein and other lipid in certain molar proportion in organic solvent to obtain lipid solution, mixing the lipid solution and buffer liquid in certain volume proportion, extruding with polycarbonate film into pellet, ultrafiltering to eliminate organic solvent to obtain blank liposome, adding alkali solution of 7-ethyl-10-hydroxycamptothecine and regulating pH value to obtain 7-ethyl-10-hydroxycamptothecine liposome. Or the 7-ethyl-10-hydroxycamptothecine liposome may be prepared through dissolving mixture of phospholipide, cholestein and other lipid in certain molar proportion in organic solvent to obtain lipid solution, spray drying and other steps. The 7-ethyl-10-hydroxycamptothecine liposome has granularity of 50-200 nm, encapsulating rate over 95 % and determined curative effect.
US20110311650 Multiplexed biomarkers of insulin resistance The invention, in some aspects, relates to methods for characterizing glucose-related metabolic disorders. In some aspects, the invention relates to methods and kits useful for diagnosing, classifying, profiling, and treating glucose-related metabolic disorders. In some aspects, the invention relates to methods useful for diagnosing, classifying, profiling, and treating diabetes.
US20060030045 Antisense modulation of c/ebp beta expression Antisense compounds, compositions and methods are provided for modulating the expression of C/EBP beta. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding C/EBP beta. Methods of using these compounds for modulation of C/EBP beta expression and for treatment of diseases associated with expression of C/EBP beta are provided.
WO2005073398A1 Method of assaying capability of inhibiting fat level increase A simple method of assaying the capability of inhibiting fat level increase that is indispensable for searching for a substance capable of inhibiting fat level increase in fat tissue. In particular, a method of assaying the capability of inhibiting fat level increase of a test substance, characterized in that the method comprises: step (1) of measuring the activity of monoacylglycerol acyltransferase in a system of monoacylglycerol acyltransferase and test substance brought into contact with each other, and step (2) of estimating the capability of inhibiting fat level increase of the substance on the basis of difference obtained by comparing the activity measured in the step (1) with reference activity.
US20100063151 Acylamide compounds having secretagogue or inducer activity of adiponectin The present invention provides acylamide compounds, prodrugs thereof, or pharmaceutically acceptable salts thereof; and an adiponectin inducer or secretagogue, and therapeutic methods by administering the same.
WO2008149154A2 Tegaserod succinate and polymorphic forms The present invention relates to various novel salts of tegaserod and to novel polymorphic forms of various salts of tegaserod, including polymorphic forms of tegaserod succinate, tartrate, malonate, camphor sulphonate, mandelate, oxalate and fumarate. The invention further relates to processes for the preparation of these novel salts and novel polymorphic forms. The invention also relates to pharmaceutical compositions comprising these novel salts or novel polymorphs, and to uses of said compositions for treating patients suffering from gastrointestinal disorders.
EP1202967B1 Sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester The present invention is directed to sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester a metabolite of the 5HT2A antagonist (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol and a processes for its preparation and its use in the treatment for a number of disease states.
WO2008098374A1 Salts, prodrugs and polymorphs of fab i inhibitors Salts of compounds according to formula (I) wherein the X is selected from the group consisting of H2SO4, HSO3R', HSO3Ar, H3PO4, HCl, HBr, CF3CO2H and CCl3CO2H. The preferred salt being the p-toluene sulfonate. These compounds and their pharmaceutical composition are useful as Fabl inhibitors for treating bacterial infections.
CN1569022A Dripping pills of lentinan and its preparing process The invention discloses dripping pills of lentinan and its preparing process, wherein the dripping pill comprises lentinan and base material, the base material can be selected from polyethylene glycol 6000, polyethylene glycol 4000, stearic acid, sodium stearate, Polyoxyethylene Stearates, glyceryl monostearate, glycerol gelatine, the condensation agent can be one or more from dimethyl silicon oil, fluid wax, rape seed oil, and tea oil.
CN102743353A Roflumilast tablet preparation and preparation method thereof The invention belongs to the technical field of medical technology and particularly discloses a Roflumilast tablet preparation and a preparation method thereof. By means of the method, active component Roflumilast and lactose are subjected to micro-powder treatment, and povidone K 90 is added in the prescription to serve as the adhesive, so that the tablet preparation is prepared. The Roflumilast tablet preparation prepared by the method is up to specification in content uniformity and obviously improved in prescription composition, disintegration time limit, a disintegration phenomenon and dissolving actions, provides a new choice for chronic obstructive pulmonary disease (COPD) patients with different sicken characteristics and meets the requirements for treating of asthma and the chronic obstructive pulmonary diseases to the largest extent.
CN101982462A Compound separated and extracted by marine fusarium and application thereof The invention designs compound separated and extracted by marine fusarium (Fusarium sp. QY010) and application thereof. The compound is the active compound which is obtained by fermenting, separating and purifying the fusarium QY010, wherein the chemical name of the active compound is 5-butyl pyridine formic acid, and the active compound is obtained by screening the pseudomonas aeruginosa screening model QSIS2 and the chromobacterium type bacterial strain CV026. Within the concentration range that the pathogenic bacteria can not be killed, the compound has the double-inhibitory action to the quorum-sensing system of the pseudomonas aeruginosa and the chromobacterium, can restrain the pathogenic behavior of the bacterial quorum sensing regulation, can obviously reduce the yield of the chromobacterium and the mycetin, can reduce the virulence factors of the quorum-sensing regulation of the pseudomonas aeruginosa, and can weaken the drug resistance of the pathogenic bacteria. The invention has the advantages of being easy to obtain the preparation raw materials, easy to ferment and cultivate the bacterial strain, high in yield, and simple and easy to control the technical process for preparing the compound. Furthermore, the analogues derived by the compound can be used for the research and the development of novel antibacterial agents.
WO2014044754A1 4-indazolylamino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer The invention provides novel indazole-substituted diaminopyrimidines of formula I, to methods of preparing such compounds, to pharmaceutical compositions containing such compounds,and to methods for using such compounds in treatment of diseases including cancer; wherein R1-R8 are as defined in the specification.
CN1628656A Armillarisin A soft capsule and preparation method thereof The invention discloses a medicinal armillarisin soft capsule and its preparation method, wherein the medicament can be added by active components including armillarisin, dissolving agent, diluent, emulsifying and solubilizing agent, anti-oxidizing agent. Each tablet of armillarisin soft capsule contains armillarisin 5-45mg, preferably 10-40mg, the dissolving agent and diluent can be used separately, or mixed by different proportion, the charging amount is 40-90%, preferably 75-85%, the emulsifying agent can be used separately, or mixed by different proportion, the charging amount is 5-20%, preferably 10-15%, the antioxidant stabilizing agent can be used separately, or mixed by different proportion, the charging amount is 1-10%, preferably 3-7%. The shell of the soft capsule can be prepared from gelatin, glycerin, sorbierite, titanium dioxide of 0.2-1.2%, preferably 0.5-0.7% of gelatine weight can be added as opacifier.
EP1605942A1 Regimen of administration for nelfinavir The invention relates to a method of treating human immunodeficiency virus (HIV) in a mammal comprising administering to a mammal in need thereof a therapeutically effective amount of nelfinavir in a pharmaceutical composition, wherein the nelfinavir is administered with food.
WO2012091534A1 Antibacterial agent for treating infectious diseases of bacterial origin The invention relates to the field of medicine and, more specifically, to an antibacterial agent for treating infectious diseases of bacterial origin, including hospital-acquired infections and drug-resistant tuberculosis, in the form of a nanostructured ionic complex synthesized from carbohydrates, proteins and/or polypeptides (albumins, interleukins, interferons, signal proteins, etc.) which, in order to enhance the antimicrobial effect in vivo through the activation of immunocompetent cells, contain at least one terminal amino acid, such as Phe, Ala, Val, Ala, Leu, He, etc., with electron donor functional groups, iodine and alkaline and alkaline-earth element halides in the fourth stage at a given ionic strength; the antibacterial agent increases the sensitivity of bacteria, including antibiotic-resistant bacteria, to antibiotics, enhances monocyte and macrophage activity and increases the effectiveness of the antibiotic treatment of hospital-acquired infections and drug-resistant tuberculosis, as well as having an antiviral effect, stimulating the haematogenic function of the bone marrow and exhibiting an antitumour effect and radioprotective properties. With the components in acceptable concentrations, the antibacterial agent can be used as a non-medicinal agent (a biologically active additive or parapharmaceutical agent). The antibacterial agent is proposed in a pharmacological form that is suitable for parenteral, oral, external or other administration, and the nanostructured ionic complex has the formula [{(Ln(MeI3)+)y[Me(Lm)I]+ x}(Cl-)y+x+k], where М = 30-300 kDa.
WO2010046321A1 Nutritional composition with anti-regurgitation properties A nutritional composition for the management of regurgitation in infants which composition includes which composition includes a protein source consisting essentially of partially hydrolysed proteins, a lipid source and a carbohydrate source comprising a starch selected from cereal starch or potato starch wherein the starch amounts to between 18 to 25% of the nutritional composition on a dry weight basis.
CN101849903A Suppository for alleviating pain The invention relates to a suppository for alleviating pain, which is prepared from fentanyl and pharmaceutically acceptable salt which are used as active ingredients and pharmaceutically acceptable auxiliary materials through a certain preparation process. The invention aims to provide a new preparation, namely, a fentanyl suppository which has the advantages of responding quickly, improving the bioavailability of medicaments, fully exerting curative effect of the medicaments, reducing adverse reaction and avoiding first pass effect of livers for patients and medical workers. The suppository is used for alleviating pain clinically.
US20110124715 Antiviral Oligonucleotides Having a Conserved G4 Core Sequence Modified oligonucleotides having a conserved G4 sequence and a sufficient number of flanking nucleotides to significantly inhibit the activity of a virus are provided. G4 quartet oligonucleotide structures are also provided. Methods of prophylaxis, diagnostics and therapeutics for viral-associated diseases are also provided.
CN103432123A Application of matrine to preparation of medicament for treating CML The invention provides application of matrine to preparation of a medicament for treating CML (chronic myelogenous leukemia), and particularly application to preparation of a medicament for treating T315I mutated CML. Researches show that the matrine has an obvious concentration-dependent apoptosis inducing effect on K562 and 32Dp210-T315I; the matrine has obvious concentration-dependent growth inhibiting and apoptosis inducing effects on CML primary cells; for normal bone marrow cells, the matrine has a low toxic effect, and can obviously concentration-dependently reduce expression of c-Myc of K562 and 32Dp210-T315I. The matrine provided by the invention has low toxicity and has tumor targeting. The invention provides the theoretical basis for searching a new therapeutic target of CML and a matrine target and enabling the matrine to enter clinical application as a medicament.
CN101284097A Plaster for curing the protrusion of lumbar intervertebral discs, hyperosteogeny and rheumatoid and preparation method thereof A plaster for treating lumbar intervertebral disc protrusion, hyperosteogeny and rheumatoid diseases is provided. The plaster contains a base drug prepared from four groups of drugs and a dusted powder drug. The base drug is prepared from rosin and mung bean; sesame oil, angelica, cochinchina momordica seed, common anemarrhena, dahurian angelica root, croton, hard clam, indian iphigenia bulb, corymbose knoxia and teasel root; frankincense, myrrh, dragon's blood, catechu, calomel, verdigris, realgar, salammoniac, arsenic trioxide, gamboge, natural indigo, mercuric oxide, calcined plaster, camphor, kansui root and borneol; and castor seed, almond, hydnocapus seed, cochinchina momordica seed and croton. The dusted powder drug is prepared from ephedra root, Chinese wild ginger, cinnamon, honey locust, raw pinellia tuber, cloven, raw arisaema and borneol. The plaster has the advantages of precise and scientifi formulation, wide raw material source, simple process, low cost, good skin permeation for the affected part, good therapeutic effect, short treatment period and quick effect, and is used for treating lumbar intervertebral disc protrusion, hyperosteogeny and rheumatoid diseases with a cure rate of 63% or higher and a total effective rate of 96% or higher.
CN102871973A Omeprazole sodium freeze-drying preparation and preparation method thereof The invention discloses an omeprazole sodium freeze-drying preparation and a preparation method thereof; the omeprazole sodium freeze-drying preparation comprises the raw materials in parts by weight: 1 part of omeprazole sodium, 0.023 part of sodium calcium edetate, 0.01-0.016 part of sodium hydroxide and 46.9 parts of water for injection. The omeprazole sodium freeze-drying preparation in the invention can be used for solving the problem that the omeprazole sodium is sensitive to metal ions, and the product is uniform and consistent in appearance and stable in quality; furthermore, the energy efficiency is reduced, and the production efficiency of the omeprazole sodium freeze-drying preparation for injection can be improved.
CN1994336A Use of basket fern polysaccharides in preparation of medicament for preventing and treating acute respiratory distress syndrome The invention relates to a method for using basket fern polysaccharide to prepare the drug that treats acute respiratory distress syndrome, wherein it extracts polysaccharide from basket fern, as 5. 72% yield; the polysaccharide content is 53. 0-58. 9%; the test has proves that polysaccharide extractive can restrain the hemocytolysis caused by typical and bypass paths, without high antibody compensation activity; the animal test has proves its protection on the lung damage caused by acute respiratory distress syndrome. The inventive polysaccharide extractive can treat acute respiratory distress syndrome and influenza.
WO2006033453A1 Activity enhancer for interferon agent It is intended to provide an activity enhancer and/or a side effect-lessening agent for an IFN agent containing glycine as the active ingredient which is an excellent activity enhancer and/or a side effect-lessening agent for an IFN agent being capable of enhancing the activity of the IFN agent and/or lessening the side effect thereof in a therapy with the use of the IFN agent. It is also intended to provide an antiviral agent, a remedy for viral hepatitis, an antitumor agent, a remedy for autoimmune diseases, a food composition and so on containing the activity enhancer and/or side effect-lessening agent for an IFN agent.
EP1487469B1 Co-beadlet of dha and rosemary The present invention provides improved beadlet formulations useful for inclusion in dietary supplements customized for improving and maintaining ocular nutrition. In particular, the improved beadlets comprise DHA (docosahexaenoic acid); rosemary and/or its components; and excipients.
WO2005095381A1 Dipeptidyl peptidase inhibitors Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising Formula (I): ##STR1## wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C=NR9; and each R1, R2, R3, R4 and R9 are as defined herein.
CN101195627B New application of benzo [C] phenanthridine and protopine in producing overriding resistant bacterium medicament The invention relates to a new application of benzo [C] phenanthridine as formula I and original tropine alkaloid for preparing anti-drug-resistant bacterial drug, wherein R1-R10, R12-R15 are hydrogen and hydroxyl groups, cycloalkyl or alkyl groups with 1-12 carbon atoms, alkox or acyloxy groups, benzyloxy, chlorine or other halide atoms, amido, methylol, aldehydo, aldehydo, acetonyl, carboxy group, mesyloxy, 4-methyl-benzene sulfonyl oxygen group, aryl sulfonyl oxygen group, biphenyl phosphine acyloxy and -OCONH2, R11 is hydrogen, methyl or oxygen atom, R5 and R6 (or R15 of the formula I), R14 and R15 are formed with double bonds, R12 or R13 and nearby N atoms are formed with double bonds, N atom can be tertiary or quaternary N type, the substituents of nearby carbons of R1-R10 can have dioxolane structure. The inventive alkaloid can effectively restrain and kill drug-resistant bacterials as MRSA and ESBLs.
WO2007038073A2 Mutations and polymorphisms of hdac11 This invention relates generally to the analytical testing of tissue samples in vitro, and more particularly to aspects of genetic polymorphisms and mutations of the HDAC11 gene. The invention provides new HDAC11 mutations and SNPs, useful in the diagnosis and treatment of subjects in need thereof. Accordingly, the various aspects of the present invention relate to polynucleotides encoding the HDAC11 mutations of the invention, expression vectors encoding the HDAC11 mutant polypeptides of the invention and organisms that express the HDAC11 mutant and polymorphic polynucleotides and/or HDAC11 mutant/polymorphic polypeptides of the invention. The various aspects of the present invention further relate to diagnostic/theranostic methods and kits that use the HDAC11 mutations and polymorphisms of the invention to identify individuals predisposed to disease or to classify individuals with regard to drug responsiveness, side effects, or optimal drug dose.
US20120149668 Glucocorticoid receptor alleles and uses thereof Provided here in are, inter alia, methods of determining whether a patient is resistant or sensitive to glucocorticoid therapy.
US20120301408 Oral care methods and compositions utilizing chitosan-derivative compounds Described herein is a method of reducing bacteria in the mouth of a subject, the method comprising contacting (e.g., rinsing) the mouth with an effective amount of a composition comprising a soluble derivatized chitosan, thereby reducing bacteria in the mouth of the subject.
US20050222387 Smac-peptides as therapeutics against cancer and autoimmune diseases The invention is directed to the use of Smac to sensitize different tumors and self-reactive immune cells to various pro-apoptosic stimuli, in that the cells subsequently undergo apoptosis. Therefore, Smac can be used as a compound for the manufacture of a medicament for the treatment of cancer and autoimmune diseases. Sensitization of the cells is achieved either by applying a cell-permeable form of Smac combined with known anticancer agents or by overexpression of the protein. It is an object of the invention to provide a new method in cancer and autoimmune disease therapy by using Smac agonists for apoptosis regulation. Thus, Smac agonists represent novel promising cancer and autoimmune disease therapeutics to potentiate the efficacy of cytotoxic therapies even in resistant tumors and immune cells.
CN101543491A Application of m-chlorobenzoyl substituted dehydrosilybin for preparing antiviral drugs The invention relates to application of m-chlorobenzoyl substituted dehydrosilybin for preparing antiviral drugs, in particular to medicinal application of a 2-3-position m-chlorobenzoyl substituted 2,3-dehydrosilybin ester derivative, namely a compound of m-chlorobenzoic acid [3-(4-hydroxy-3-methoxyphenyl)-6-(3,5,7-trihydroxy-4-oxo-chromene-2)-2,3-dihydro-1,4-benzodioxane-2]-methyl ester or a pharmaceutical salt thereof in the preparation of medicaments for controlling viral infections and/or oral ulcers caused by herpes simplex virus HSV-1. The compound is prepared by semi-synthesis of a chemical method, and pharmacological experiments show that the compound has definite inhibition on the herpes simplex virus HSV-1, and the half inhibition concentration IC50 value is 44.78 micrograms per milliliter.
WO2007040440A1 New pyrimidine derivatives and their use in therapy as well as the use of pyrimidine derivatives in the manufacture of a medicament for prevention and/or treatment of alzheimer’s disease The present invention relates to use of compounds of formula (I) as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, as pharmaceutical ingredients for treatment of dementia, Alzheimer's Disease, Parkinson's Disease, Frontotemporal dementia Parkinson's Type, Parkinson dementia complex of Guam, HIV dementia, diseases with associated neurofibrillar tangle pathologies and/or dementia pugilistica .
US20110130367 Combination Therapy for Treating Proliferative Diseases The present invention relates generally to new chemical combinations and methods for their use in the treatment of proliferative diseases and in particular cancer.
US20090169619 Carbamazepine extended release dosage form Extended release pharmaceutical dosage forms of carbamazepine for oral administration to maintain a patient's blood concentration for at least a 12 hour period, methods of administering dosage forms and processes for the preparation of such dosage form.
EP0879281B1 Methods for transforming dendritic cells and activating t cells Recombinant dendritic cells are made by transforming a stem cell and differentiating the stem cell into a dendritic cell. The resulting dendritic cell is an antigen presenting cell which activates T cells against MHC class I-antigen targets. Kits, assays and therapeutics are based upon the activation of T cells by the recombinant dendritic cell. Cancer, viral infections and parasitic infections are all ameliorated by the recombinant dendritic cells, or corresponding activated T cells. Therapeutic compositions and pharmaceutical compositions are provided.
EP2027082A1 12-aryl or heteroaryl prostaglandin analogs A compound having structure (I) is disclosed herein. Compositions, medicaments, and therapeutic methods related thereto are also disclosed.
CN102836128A Method for preparing ultrafine particles of water-insoluble or insoluble medicine The invention discloses a method for preparing ultrafine particles of a water-insoluble or insoluble medicine. The method mainly comprises the following steps: dissolving the water-insoluble or insoluble medicine into other solvents to prepare a medicine solution; allowing the medicine solution to enter an aqueous solution, into which a stabilizing agent is dissolved, through a dispersing film to form a solution on which ultrafine medicine particles are suspended; and drying the solution on which ultrafine medicine particles are suspended to obtain the product. The invention also discloses the ultrafine medicine particles prepared by the method. By the method, the particle size range of the medicine particles can be controlled precisely. The method has the characteristics of simple process, low cost and environmental friendliness and meets the requirement of industrialized production.
CN103189369A Pyridinones/pyrazinones, method of making, and method of use thereof Pyridone and pyrazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
CN1679538A Oral preparation of diterpene compounds against cancers and preparing method and use thereof An orally taken anticancer diterpenoid medicine is prepared from the diterpenoid as anticancer component and the composite solvent composed of polar solvent, semi-polar solvent, surfactant, high-molecular dispersing solid carrier, NaCl, glucose, flavouring and water through dissolving.
WO2012120052A1 Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof The invention relates to the compounds of formula (I) and physiologically acceptable salts thereof. The compounds are suitable, e.g., for treating hyperglycemia.
US20070299065 Tetrahydropyran Derivatives as Antidiabetics Novel compounds of the formula (I), in which T, E, R, R′, R″, R1, R2 and R2′ have the meanings indicated in patent Claim 1, are suitable as antidiabetics.
US20090042869 SIGNAL-DEPENDENT SPLICING OF TISSUE FACTOR PRE-mRNA IN PLATELET CELLS The invention relates to therapeutic target recognition, development, and validation of a compound capable of directly or indirectly modulating TF pre-mRNA splicing in a platelet cell and the use of a platelet TF pre-mRNA splicing modulator for the treatment of a subject suffering from, or thought to be suffering from, disordered coagulation.
CN101843588A Biphenyl dimethylesterate nano lipid carrier and preparation method thereof The invention discloses a biphenyl dimethylesterate nano lipid carrier, mainly prepared by biphenyl dimethylesterate, solid lipid material, liquid lipid, water soluble emulsifier, lipid soluble emulsifier and water for injection. The preparation method thereof includes: (1) the biphenyl dimethylesterate, solid lipid material, liquid lipid and lipid soluble emulsifier are dissolved into organic solvent when being heated, so as to form an organic phase; (2) the water soluble emulsifier and additive are dissolved into the water for injection, heating is carried out, so as to form a water phase; (3) the organic phase is injected into the water phase while stirring, stirring is carried out until the organic solvent is completely volatilized, thus obtaining primary emulsion; (4) the primary emulsion is poured into iced water, and stirring is carried out, thus obtaining the biphenyl dimethylesterate nano lipid carrier. The biphenyl dimethylesterate nano lipid carrier of the invention has good biocompatibility, is easy to degrade, reduces toxic and side effect of biphenyl dimethylesterate and improves tolerance of organism.
EP2480532B1 Piperidine derivatives and their use to treat obesity, diabetes, dyslipidemia and atherosclerosis Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1, R2, R3 and R4 have the significance given in claim 1.
US7297684 breast and prostatic tumors; administration of an antisense oligodeoxynucleotide which is complementary to a portion of the gene encoding insulin-like growth factor binding protein -5 A method is provided for treating hormone-regulated tumors (for example, breast and prostatic tumors) in mammals, including humans, by administration of an antisense ODN which is complementary to a portion of the gene encoding IGFBP-5. Using the Shionogi tumor model in vitro and in vivo, the administration of such an ODN was shown to reduce proliferation of tumor cells, and also to delay the progression to androgen independence. Thus, treatment of prostate cancer in mammals, including humans, and delay of the progression of prostate tumors to androgen independence is accomplished by administering to the mammal a therapeutically effective amount of an antisense oligodeoxynucleotide which is complementary to a portion of the nucleic acid sequence encoding IGFBP-5 and which hybridizes with such a sequence to inhibit expression of IGFBP-5. Specific antisense ODN's which are suitable for use in the method are GACCACGCTGATCACCAT (Seq. ID. No. 1), which is derived from the murine gene sequence, and CGCGGTGAGCAACACCAT (Seq. ID. No. 3) and AGGTCATGCAGCAGCCGC (Seq. ID No 4), which are derived from the human gene sequence.
US20070105936 new crystals forms of Sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate; VLA-4 (very late antigen-4) inhibitor; therapeutic drug for disorders caused by cell adhesion; water soluble, stability The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate.
US7342022 Compounds in the treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3 The present invention relates to new compounds of formula I wherein R1, R2, R3, n, m are defined as in claim 1, a process for their preparation and new intermediates used in the preparation thereof, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, especially in the prevention and/or treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3
US20140056927 Lipotheichoic acid from lactic acid bacteria and its use to modulate immune responses mediated by gram-negative bacteria, potential pathogenic gram-positive bacteria The invention relates to a composition for modulating the immune responses induced by Gram negative bacteria, potential pathogenic Gram positive bacteria and/or their derivatives, comprising lipoteichoic acid from lactic acid bacteria as an active ingredient. It also relates to the use of a lipoteichoic acid from lactic acid bacteria as an active ingredient and/or lactic acid bacteria producing it and/or its supernatant of culture, in the manufacture of a medicament, an oral or topical product for cosmetic, dermatological or opthalmological applications, a food or petfood composition for modulating bacterial colonisaion, immune responses and decreasing the inflammatory processes, associated with bacterially mediated disease and infection in the gastrointestinal tract, bone, skin, eye, ear, lung and rectal cavity. The invention also relates to lipoteichoic acid selected thereof.
CN101933938A Sustained-release in-vivo pathogen killing agent and preparation and using methods thereof The invention relates to a sustained-release in-vivo pathogen killing agent and preparation and using methods thereof, which belong to the technical field of medicaments. The pathogen killing agent comprises the following components: aqueous solution of sodium chlorite serving as an agent A, aqueous solution of citric acid serving as an agent B or 3 to 5 percent acetic acid or vinegar. A preparation process comprises the following steps of: recrystallizing a commodity, namely, sodium chlorite to remove harmful impurities, mixing the recrystallized sodium chlorite and water to obtain aqueous solution, refrigerating the aqueous solution and removing a chlorate impurity by filtering; and mixing the aqueous solution of sodium chlorite and aqueous solution of citric acid or acetic acid according to proportion and adding water into the mixture for drinking. After being taken, the pathogen killing agent can continuously supply chlorine dioxide into bodies so as to selectively kill multiple in-vivo pathogens such as bacteria, viruses, protozoa, fungi, parasites and the like. The pathogen killing agent is used for treating patients suffered from difficult miscellaneous diseases, has the advantages of safety, high efficiency, low price and easy popularization and fills the blank of the treatment of human diseases by using chlorine dioxide in China.
WO2007077309A1 Combination comprising combretastatin and anticancer agents An antitumour combination comprising a stilbene derivative and an anticancer compound chosen from VEGF inhibitors, and more particularly VEGF Trap. Also provided are methods for using these pharmaceutical preparations for the treatment of solid carcinomas and the like.
CN1985949A Slow released capsule of cefradine and bletilla tuber glue for animal and birds The present invention belongs to the field of veterinary medicine technology, and is especially slow released veterinary medicine capsule prepared with cefradine and bletilla tuber as material. The preparation process includes the following steps: water extracting and alcohol precipitation to extract bletilla tuber glue; mixing cefradine and bletilla tuber in the ratio of 1 to 3 and 10 % concentration alcohol solution of PVP as adhesive; making pellet of 20 meshes and encapsulating. The slow released veterinary medicine capsule has long medicine retaining time in the disease focus, high local medicine concentration, excellent bioadhesion and obvious medicine slow releasing characteristic.
US20100144708 Heterocyclic compounds containing nitrogen atoms or pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical composition comprising the same for treatment of cancer The present invention relates to new heterocyclic compounds containing nitrogen atoms or pharmaceutically acceptable salts thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same for treatment of cancer. The compounds according to the present invention induce DNA damage due to reactive oxygen species to activate c-abl and p53, induce RhoB to generate apoptosis, and induce cell death by down-regulating Bcl2 involved in cell survival, which is generated by dysregulated signals via the mitochondria pathway, thereby inhibiting tumor cell growth and inducing apoptosis. Accordingly, the composition according to the present invention can be used to treat cancer.
CN102846681A Medicament for treating livestock diarrhea The invention discloses a medicament for treating livestock diarrhea. The medicament comprises effective components of, by weight, 6 to 10 parts of valeriana jatamansi and 1 to 3 parts of norfloxacin. The medicament for treating livestock diarrhea is scientific and reasonable in formula, short in anti-diarrheal time and rapid in effect producing; has good broad-spectrum antibacterial and antiviral effects, can enhance immunities effectively, and has no toxic and side effects and medicament residue; and is low in production cost and convenient to use.
US20120177599 Compositions and methods for treatment, diagnosis and prognonis of mesothelioma Described herein are compositions and methods for the treatment and diagnosis of mesothelioma, and determination of prognosis of mesothelioma patients after surgical operation. Specifically, the invention relates to microRNA molecules associated with treatment, diagnosis and determination of prognosis of mesothelioma, as well as various nucleic acid molecules relating thereto or derived therefrom.
CN101019841A Prepn process and application in medicine for treating liver fibrosis of curcumin The present invention relates to preparation process and application in medicine for treating liver fibrosis of curcumin. The medicine treating liver fibrosis has curcumin as main effective component and pharmaceutically acceptable carrier, such as excipient, additive and flavoring agent, and may be prepared into different forms, including medicine powder, tablet, micro pill, etc. Curcumin has obvious effect of treating liver fibrosis, no obvious toxic side effect and rich resource.
CN1840015A Medicinal composition for treating psoriasis The invention discloses a pharmaceutical composition for treating psoriasis, which comprises the following constituents (by weight portions): subprostrate sophora root 90-150 parts, wofberry bark 90-150 parts, natural indigo 30-60 parts, pangolin scales 30-60 parts, licorice root 20-80 parts, atractylodes rhizome 100-200 parts, borneol 20-50 parts, and ledebouriella root 30-60 parts.
US20100239645 Methods and Compositions for Wound Healing Glycerophosphate salts have been found to hasten the healing of wounds and minimize the formation of scars, particularly when it is first applied to a wound about 0 to about 7 days after the wound is inflicted. Methods and compositions are provided for treating wounds using a composition comprising an effective amount of glycerophosphate salt. In particular, methods are provided for treating wounds using calcium glycerophosphate (CGP), for accelerating the healing process, reducing pain and scar formation, and for the cosmetic reducing, excision, erasure and/or complete repair of scars (scar revision).
US7345046 Using quinazoline type compound ; antiproliferative agents Heteroaryl-fused pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the heteroaryl-fused pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the heteroaryl-fused pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.
CN103393670A Application of Chukrasone B in preparing anti-hypoxic medicines The invention discloses an application of Chukrasone B in preparing anti-hypoxic medicines. According to the invention, the anti-hypoxic effect of Chukrasone B is observed through integral and cellular hypoxic models. The results show that Chukrasone B can remarkably improve the survival rate and the survival time of mice with asphyxial hypoxia and acute decompressed hypoxia, alleviate myocardial damage of medicine specificity hypoxic mice and further has a remarkable protective effect on hypoxia injury of cardiac myocytes and nerve cells of neonatal rats cultured in vitro. The invention provides a use of Chukrasone B in preparing anti-hypoxic medicines.
WO2006133498A1 Acid addition salts of n-ethyi-n'-[2-methoxy-4-(5-methyi-4-{[(1s)-1-pyridin-3-ylbutyi]amino}pyrimidin- 2-yl)phenyl]urea and uses thereof The present invention provides an acid addition salt of N-ethyl-N'-[2-methoxy-4-(5-methyl-4-{[(1S)-1-pyridin-3-ylbutyl]amino}pyrimidin-2-yl)phenyl]urea and uses thereof including a method for the treatment of a hyperproliferation-related disorder. The present invention also provides a pharmaceutical composition comprising an acid addition salt of N-ethyl-N'-[2-methoxy-4-(5-methyl-4-{[(1S)-1-pyridin-3-ylbutyl]amino}pyrimidin-2-yl)phenyl]urea.
CN102491935A Nitrobenzaldehyde indole schiff base, preparation method and application thereof The invention relates to a nitrobenzaldehyde indole schiff base, a preparation method and application thereof. The schiff base has a structural formula shown as (I), (II) or (III), and a substituent R is -NO2. The preparation method comprises steps of: placing a solvent of ethanol in a reactor and adding nitrobenzaldehyde; adding amino indole compound with a same molar amount as the nitrobenzaldehyde; dissolving completely and controlling a temperature at 60-80 DEG C, heating for reflux and reacting for 4-8 h; and evaporating solution in the reactor to obtain a crude product and recrystallizing to obtain a finished product. The product of the invention can effectively inhibit propagation of a plurality of tumor cell strains and has good water-solubility.
WO2010111406A3 Purine derivatives useful as anti - cancer agents The invention relates to compounds of formulae I or II, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.
WO2014079840A1 Use and application regimen of a pharmaceutical composition containing levonorgestrel and a cox inhibitor for on-demand contraception The invention relates to a method for hormonal female controlled on-demand contraception, wherein a pharmaceutical preparation containing a COX inhibitor and levonorgestrel is taken on-demand before expected sexual intercourse. The invention further relates to pharmaceutical compositions and an application regimen for on-demand contraception.
WO2011058582A1 Histone deacetylase inhibitors for the treatment of fungal infections Described are bridged compounds of the formula (I), their analogs, tautomeric forms, stereoisomers, geometrical isomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. The invention relates to compositions and methods to treat fungal infection. These compounds are selective HDAC inhibitors that act as inherent antifungal compounds or enhance the activity of other antifungal compounds such as azoles.
CN101104629A Dicycloglycosides compound, preparation method and application thereof Disclosed is a preparation method of a bicyclol glycoside compound, which is characterized in that first bicyclol and glycine protected by Fmoc are condensed under the catalysis of 1-(3-dimethylamino propyl)-3-ethyl carbodiimide hydrochloride and 4-dimethylamino pyridine, and then protecting group of Fmoc is removed under the effect of acetonitrile diethylamine to obtain intermediate bicyclol-glycine ester which is the condensation of the bicyclol and the glycine. At last, Alpha or Beta glycosyl carboxyl methyl glycoside of glucose, galactose, mannose, allose, altrose, gulose, idose, talose, acetyl-glucosamine or acetyl galactosamine has condensation reaction with the intermediate bicyclol-glycine ester in solvent N-methyl pyrrolidone and under the effect of condensing agent and alkali. The water solubility of the bicyclol can be increased with the invention, and the bioavailability of the bicyclol is improved, which can provide enough raw material and effective compound route for the study of the anti-hepatitis drug. The invention has the advantages that the preparation method is simple and convenient; the condition is easy to control.
CN101690723B Sumatriptan succinate compound preparation and preparation method thereof The invention discloses a sumatriptan succinate compound preparation, which comprises sumatriptan succinate pellets and naproxen sodium pellets; the active components in part by mass are 119 parts of sumatriptan succinate and 500 parts of naproxen sodium. The sumatriptan succinate pellets comprise 87 to 97 weight percent of medicament-containing pellet core, 1 to 5 weight percent of isolation layer and 2 to 8 weight percent of coating layer; and the naproxen sodium pellets comprise 99 to 99.9 weight percent of medicament-containing pellet core and 0.1 to 1 weight percent of isolation layer. Amethod for preparing the preparation comprises the following steps: respectively preparing the umatriptan succinate pellets and the naproxen sodium pellets; and mixing the umatriptan succinate pellets and the naproxen sodium pellets to prepare pharmaceutically acceptable formulation. The two medicaments in the compound preparation form a special independent release curve in the dissolving-out process so as to achieve the aim that the naproxen sodium is firstly released and absorbed and then the sumatriptan succinate is released and absorbed and further achieve better treatment effect.
US20100216835 Method For Modulating Microbial Quorum Sensing The present invention provides compositions and methods for modulating bacterial quorum sensing using antagonist or agonist compounds. Further, the present invention provides methods of treating or preventing microbial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.
CN102079703A Method for preparing novel nonsteroidal anti-inflammatory drug and anti-inflammatory and analgesic effects thereof The invention relates to a compound obtained by esterifying carboxylic acid-containing nonsteroidal anti-inflammatory drugs with paeonol and nor-paeonol, a preparation method and application thereof. The compound is obtained by taking the carboxylic acid-containing nonsteroidal anti-inflammatory drugs such as ibuprofen and the like as a raw material and esterifying the raw material with the paeonol through sulfonyl chlorination or with the nor-paeonol by a carbimide method. The compound has anti-inflammatory, and antipyretic and analgesic effects.
US20110212053 Phosphatidylinositol 3 kinase inhibitors Provided are compounds according to Formula (I): or stereoisomer, prodrug, polymorph, or pharmaceutically acceptable salt forms thereof, wherein X, Y, R1, R6, R7, and R8 are as defined, and which compounds are effective inhibitors of PI3-kinase and/or other medically and clinically relevant kinases. Also provided are pharmaceutical compositions and methods of using the compounds and compositions as PI3-kinase and kinase inhibitors. More particularly, the compounds of the invention provide treatments and therapeutics for human diseases regulated by, or associated with, the activity of, PI3-kinases and/or protein kinases, or mutant or variant forms thereof.
EP2686306A1 Benzo [b][1, 4]oxazin derivatives as calcium sensing receptor modulators Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).
US20110318432 Compositions for the treatment of gastro-esofageal reflux disease (gerd) Oral pharmaceutical, nutraceutical, health foods and medical device compositions based on polysaccharides from Opuntia Ficus Indica cladodes in combination with other active substances are useful for the prevention or treatment of GERD (Gastro-Esophageal Reflux Disease), gastric esophagitis and related diseases (e.g. dyspepsia, esophagitis, esofageal tumour, gastro-intestinal symptoms, chronic pharyngitis, Barrett's esophagus, esophageal adenocarcinoma, GERD-related pulmonary symptoms).
US20050171354 Heterocyclic amines such as (2S,3S)-3-((1R)-6-methoxy-1-methyl -1-trifluoromethylisochroman-7-yl)methylamino-2-phenyl piperidine, used as analgesics, antiinflammatory agents, or for prophylaxis of cardiovascular disorders This invention provides a compound of the formula: and its pharmaceutically acceptable salts, wherein R1 is C1-C6 alkyl; R2 is hydrogen, C1-C6 alkyl, halo C1-C6 alkyl or phenyl; R3 is hydrogen or halo; R4 and R5 are independently hydrogen, C1-C6 alkyl or halo C1-C6 alkyl; and n is one, two or three. These compounds are useful as analgesics or anti-inflammatory agents, or in the treatment of cardiovascular diseases, allergic disorders, angiogenesis, CNS disorders, emesis, gastrointestinal disorders, sunburn, urinary incontinence, or diseases, disorders or adverse conditions caused by Helicobacter pylori, or the like, in a mammalian subject, especially humans. Intermediates for preparation of the compounds of Formula (I) are also disclosed.
WO2006038603A1 Phosphate ion adsorbent Disclosed is a phosphate ion adsorbent containing a polymer or a salt thereof to which a metal complex group represented by the general formula (II) below is bonded directly or via a spacer. The phosphate ion adsorbent specifically adsorbs phosphate ions in a living body and has a high adsorption capacity for phosphate ions. Consequently, this phosphate ion adsorbent is useful for removing phosphate ions from a living body.
US20110262383 Naphthalimide Dosing by N-Acetyl Transferase Genotyping The present invention provides methods for dosing patients with naphthalimides, including amonafide, amonafide salts, and analogs thereof based on N-acetyl transferase genotyping. The invention also provides methods for dosing the amount of granulocyte colony stimulating factor (GCSF) used in combination with naphthalimide to prevent or modulate leukocytopenia.
US20110257253 Preparation method of polymeric micellar nanoparticles composition containing a poorly water-soluble drug Provided is a method for preparing a poorly water-soluble drug-containing polymeric micellar nanoparticle composition, which includes: dissolving a poorly water-soluble drug, a salt of polylactic acid or polylactic acid derivative, whose carboxylic acid end is bound to an alkali metal ion, and an amphiphilic block copolymer into an organic solvent; and adding an aqueous solution to the resultant mixture in the organic solvent to form micelles, wherein the method requires no separate operation to remove the organic solvent prior to the formation of micelles. The method for preparing a poorly water-soluble drug-containing polymeric micellar nanoparticle composition is simple, reduces the processing time, and is amenable to mass production.
US20110207697 Xanthohumol compositions and methods for treating skin diseases or disorders The present invention features therapeutic and prophylactic compositions comprising xanthohumol and/or xanthohumol/cyclodextrin complexes and methods of using such compositions for treating a skin condition, disease, or disorder.
CN101313914A Uses and preparations of common camptotheca fruit glycosides of common camptotheca fruit extract The invention discloses an application of vincoside lactam extracted from common camptotheca fruit in preparation of antibacterial or antiviral or anti-hyperthermia or anti-inflammatory or pain relieving drugs or in preparation of drugs for treating infectious diseases caused by sensitized bacteria and viruses or leptospirosis. The diseases caused by sensitized bacteria and viruses comprise: acute tonsillitis, faucitis, upper respiratory tract infections, bronchitis, otitis media pneumonia, conjunctivitis, hordeolum, periodontal abscess, burn wound infections, urinary tract infections, and infections caused during after-surgery prevention. The invention also discloses a vincoside-lactam preparation with the application.
US8007781 Molecular vaccine linking an endoplasmic reticulum chaperone polypeptide to an antigen This invention provides compositions and methods for inducing and enhancing immune responses, such as antigen-specific cytotoxic T lymphocyte (CTL) responses, using chimeric molecules comprising endoplasmic reticulum chaperone polypeptides and antigenic peptides. In particular, the invention provides compositions and methods for enhancing immune responses induced by polypeptides made in vivo by administered nucleic acid, such as naked DNA or expression vectors, encoding the chimeric molecules. The invention provides a method of inhibiting the growth of a tumor in an individual. The invention also provides novel self-replicating RNA virus constructs for enhancing immune responses induced by chimeric polypeptides made in vivo.
CN101181623B Method for preparing alcohol extraction of white vein ointment The invention provides a novel preparation method for Tibetan medical white vein ointment. The invention is based on the primary prescription of Tibetan medical white vein ointment and combined with modern advanced technique, thereby the effective components of the active substances and medical materials can be effectively remained, and the contents of finished medicine and the dissolution rate of the components of crude medicines can be greatly increased, meanwhile, the the biological utilization degree is enhanced as well, thus the treatment effect is improved and the the shortcomings of the traditional white vein ointment are overcomed. The product produced by the invention has no odor and good stability, and is easy for using, carrying and storing. Besides, the invention has the advantages of simple technique, easy operation, stable source of the raw materials and auxiliary materials, and easy industrialization.
CN1981750B Soluble A-SH CoA-SH Q10 composition and its production method A water-soluble coenzyme Q10 composition for treating cardiovascular disease, hepatitis and hypoimmunocompetence is proportionally prepared from coenzyme Q10, gamma-cyclodextrin, alditol and disintegrant through high-speed stirring in water or ultrasonic oscillating, high-pressure homogenizing, freeze-drying, and granulating.
EP1482948B1 Continuous sulfatase inhibiting progestogen hormone replacement therapy ABSTRACTA method of hormone replacement therapy is disclosed comprising the step of adminstering continuously to a post-menopausal or estrogen deficient female in need of such therapy a combination of estrogen in an effective hormone replacement amount and a progestogen which is a potent sulfatase inhibiting progestogen in an amount which is both an effective endometrium protective amount and an effective breast protective amount.
US20110086921 Novel Polymorphic Forms of (4--2-Methylphenyl)Carbonyl]Amino}-3-Methylphenyl)Acetic Acid Polymorphic forms 1 and 2 of (4-{[(5-{[(3-chlorophenyl)methyl]oxy}-2-methylphenyl)carbonyl]amino}-3-methylphenyl)acetic acid, pharmaceutical compositions comprising such polymorphs and the use of such polymorphs in medicine.
WO2012144405A1 Method for producing adhesive patch, and adhesive patch A method for producing an adhesive patch comprising a supporting body layer and an adhesive layer, which comprises a step for forming the adhesive layer with use of an adhesive layer composition that is obtained by mixing an alkali metal diacetate salt, a medicament and a nonaqueous adhesive base so that the molar ratio of the medicament to the alkali metal diacetate salt ([the mole number of the medicament]:[the mole number of the alkali metal diacetate salt]) is from 1:0.5 to 1:15.
CN103102349A Protein kinase inhibitor and composition and application thereof The invention relates to compounds as shown in the general formula (I), pharmaceutical compositions containing the compounds, a method for treating diseases and disease symptoms related to abnormal activity of protein kinase by using the compounds, and medicinal use of the compounds.
US20070249622 Nicotinic receptor agonists and analogues and derivatives thereof for the treatment of inflammatory diseases This invention relates to the use of nicotine receptor agonists or analogues or derivatives thereof for treating inflammatory pulmonary diseases. Such agonists have fewer side effects than other anti-inflammatory drugs, such as steroids. Moreover, these agonists can be used alone or in combination with other anti-inflammatory drugs to alleviate pulmonary diseases.
US20130125882 Method and composition for treating asthma and copd A pharmaceutical composition and method for the treatment of asthma or other respiratory disease by inhalation from a pressurized metered dose inhaler (pMDI), a dry powder inhaler (DPI) or nebulizer, the composition and method being based on a combination of a short acting beta agonist (SABA) and an inhaled corticosteroid (ICS) in a form adapted to be delivered for inhalation from the pMDI, DPI or nebulizer.
CN1813757A Vardenafil dropping pill and its preparing method The present invention relates to a kind of vardenafil dripping pill and its preparation process. It is made up by using vardenafil and dripping pill matrix through a certain preparation process. Said vardernafil dripping pills can be used for curing male erection dysfunction, its bioavailability is high and medicine stability is good.
US20080033042 Urea-and urethane-substituted acylureas, process for their preparation and their use The invention relates to urea- and urethane-substituted acylureas and to their physiologically tolerated salts and physiologically functional derivatives. In particular, the invention relates to the compounds of the formula I wherein the radicals have meanings described herein, and to their physiologically tolerated salts and to processes for their preparation. The compounds are suitable for example as antidiabetics.
US7655688 Fused cyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
US6884807 3-bicyclic carbocyclic group substituted quinuclidine derivatives, which are cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptor and transporters This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
WO2008063232B1 Substituted pyrazolopyrimidines The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).
CN1785415A Xingnaojing injection agent for refreshment and its preparation method A í‹XingnaojingíŒ injection in the form of nano-microemulsion, subnano-emulsion, or lipid for clearing heat and reducing fire, cooling blood and detoxicating, and inducting resuscitation and refreshing brain, and its preparing process are disclosed.
WO2010122538A1 Pharmaceutical compositions for treatment of hcv patients that are non-responders to interferon The present invention provides compositions and methods of treatment of HCV infected subjects that are not sensitive to Interferon treatment. Further, compositions and methods are provided for prevention of organ transplant rejection. The compositions of the invention comprise an anti microRNA-122 oligonucleotide, and are made for administration to a primate.
EP2440213A1 Use of 1,25-dihydroxyvitamine d3 glycoside in lactating animals. The invention relates to the use of leafs comprising 1,25-dihydroxyvitamin D3 glycoside for the preparation of a composition for a single peroral administration with a density of at least 1.25 kg/I, which effects a delayed release of 1,25-dihydroxyvitamin D3 glycoside with the purpose of preventing a symptom selected from reduced appetite, paralysis or a combination of both with an animal after having given birth. The invention further relates to the composition.
CA2281496C New hydroxy derivatives of tylosin and process for their preparation The present invention relates to 12,13-dihydroxy derivatives of tylosin, new semisynthetic compounds of the macrolide class, and to a process for their preparation. According to the present invention by the oxidation of 13-hydroxy derivative a 12,13-dihydroxy compound is obtained, which can be subsequently subjected to a series of reactions such as oximation, reduction (catalytic, electrochemical) or hydrolysis yielding corresponding dihydro or tetrahydro 12,13-dihydroxy derivatives. The 12,13-dihydroxy derivatives of tylosin are represented by the formula (I) (see formula I) wherein R represents O, R1 represents CHO, CH=NOH or CH(OCH3)2, R2 represents Hor mycarosyl, R3 represents N(CH3)2 or NO(CH3)2, and - - - line represents a single or a double bond, with the proviso that when - - - line represents a single bond then R3 only represents N(CH3)2; or wherein R represents NOH, R1 represents CHO or CH(OCH3)2, R2 represents H or mycarosyl, R3 represents N(CH3)2 or NO(CH3)2, and - - - line represents a single or a double bond, with the proviso that when - - - line represents a single bond then R3 only represents N(CH3)2.
EP1470138B1 Mmp inhibitors Novel compounds according to formula I n is 0, 1, 2 or 3; X represents hydroxamic acid (CONHOH), carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group;R2, R10 and R11 independently represent hydrogen or (Cl_8)alkyl, (CZ_6)alkenyl, (C3_$)cycloalkyl, aryl(Co_6)alkyl or heteroaryl(Co_6)alkyl, all of which may optionally be substituted; R3 and R4 independently represent hydrogen, hydroxy or alkoxy; provided that if A, A', Z and R5 are all bonds, and s and t are both 0 (zero), then R6 is different from hydrogen, and that at least one of R3, R4, R10 and R11 is different from hydrogen; or a salt, hydrate or solvate thereof; pharmaceutical compositions comprising said compound; therapeutical methods comprising administering said compounds; and the use of said compounds in the manufacture of medicaments.
US20090170917 Acid Mimic Compounds for the Inhibition of Isoprenyl-S-Cysteinyl Methyltransferase Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g., Parkinson's disease).
WO2012017028A1 A novel crystalline compound comprising saxagliptin and phosphoric acid The present invention refers to a crystalline compound comprising a mixture of a compound of formula (I) (INN: Saxagliptin) and phosphoric acid or a hydrate thereof, wherein the molar ratio of the compound of formula I and the phosphoric acid is in the range of from 1:0,8 to :1,2, as well as a process of obtaining the same.
CN102379890A Anti-bacterial agents for treating childhood infections and infectious diseases and preparing method thereof The invention relates to anti-bacterial agents for treating childhood infections and infectious diseases, which adopt erythromycin ethylsuccinate, sucrose powder, sodium alginate, steviosin, hydroxy propyl cellulose, sodium lauryl sulphate, tartrazine, orange essence and sodium carboxymethyl starch as raw materials. The preparation method comprises the following steps: 1) firstly screening the erythromycin ethylsuccinate, the sucrose powder and the steviosin, then mixing uniformly, later adding the sodium alginate, the hydroxy propyl cellulose, the sodium lauryl sulphate, the tartrazine and the sodium carboxymethyl starch in turn, then uniformly mixing and crushing as fine powder for further use; 2) adding the fine power obtained in the step 1) to a right amount of dilute ethanol liquor, then fully stirring to obtain soft material, and screening by a 30 meshes sieve to obtain wet particles; 3) drying the wet particles at 45 degrees centigrade, pelletizing by the 30 meshes sieve, adding the orange essence, uniformly mixing and packaging to prepare the dry suspension. The invention has unified specification, easily grasps the dosage, dose not limit the water quantity, can be conveniently carried and used, can be applied to children tastes and has obvious curative effects.
US7652010 Azabicyclic aryl derivatives and their medical use Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile, the compounds may be used for the treatment of various diseases or disorders, including those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
CN101897968A Compound preparation for treating dyslipidemia The invention discloses a compound preparation for treating dyslipidemia. The preparation comprises the following components: hawthorn flavonoids and any one of HMG-COA reductase inhibitors. The preparation has the advantages that: medicaments are combined to fully produce complementary and synergetic effects , which contributes to thoroughly adjusting dyslipidemia and reducing the adverse reaction associated with the increase of a certain dosage; and the compound preparation prepared by combining the effective ingredients of a natural plant medicament, namely hawthorn flavonoids, and other lipid-lowering chemical medicaments can reduce TC, LDL-C and TG, increase HDL-C, and effectively adjust dyslipidemia to make the lipid level reach a standard. The compound preparation of the invention has the characteristics of short treatment course, quick effect, low side effect and low cost.
CN101323604A Novel PPAR alpha/beta dual agonist, preparation and use thereof The invention provides a new compound and a medical composition which contains the compound or the pharmaceutically acceptable salts of the compound and provides a preparation method thereof. The compound has the activity of PPAR Alpha/Gamma dual agonist in PPARs and can be used for preparing medicines for curing diseases of animals including human beings, such as diabetes, hyperlipemia, hypercholesterolemia, hypertension, atherosclerosis, coronary heart disease, obesity, metabolic syndrome and tumors.
US7247610 Suppression tumor growth Disclosed are methods for treating cancer by administering an inhibitor of the interaction of glutamate with the KA receptor complex.
CN1785180B Method for detecting compound bismuth potassium citrate metronidazole The invention provides a quality control method for a compound bismuth potassium citrate-metronidazole preparation, which includes characteristics, identification, part or all of content determination item; wherein the identification includes the characteristic reaction with sodium hydroxide and deluted hydrochloric acid, and with lead acetate, and the depositing reaction with perchloric acid, and the content determination includes taking the metronidazole as the reference substance, and taking the vitamin B6 as the reference substance, and measuring the contents of the bismuth potassium citrate by using the titrimetry. Compared with the prior art, the invention adds the content determination of the vitamin B6, and adopts the high performance liquid chromatography to measure the content of the metronidazole and vitamin B6 in the preparation, has advantages of good separation effect, and sensitive and accurate or the like; improves the quality control standard of the compound bismuth potassium citrate-metronidazole preparation, thereby ensuring the clinic curative effect of the preparation.
WO2007088473A2 Treatment and prevention of depression with pain, depression secondary to pain, and of neuropathic pain In accordance with the present invention, it has been discovered that compounds exhibiting activity as a potent noradrenaline reuptake inhibitor (e.g., a NA: 5HT ratio of greater than or equal to about 1000:1), and activity at the dopamine D2 receptor sites (e.g., lofeprarnine) are effective in the treatment and prevention of various diseases and disorders associated with noradrenaline reuptake, such as pain predominant-type depression, depression secondary to chronic or neuropathic pain, and neuropathic pain itself.
WO2010086454A9 N-(phenyl or pyridyl)prenylamine derivatives for the treatment of obesity, diabetes, cardiovascular diseases and other adiponectin-related diseases The invention relates to the use of a compound of formula (I) its pharmaceutically acceptable salts and/or solvates, in the preparation of a medicinal product for the treatment of a disease presenting altered adiponectin levels or in which it is necessary to alter the adiponectin levels.
EP0920316B1 Treatment of manic disorders The invention relates to the use of tiagabine or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of psychotic disorders.
US20080102070 SCDs As Modifiers of the p53 Pathway and Methods of Use Human SCD genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of SCD are provided.
US20080306074 Compositions Comprising Addl Receptors, Related Compositions, and Related Methods Disclosed and claimed herein are compositions comprising ADDL receptors, related compositions, and related methods. ADDL receptors are typically, but perhaps not exclusively, localized at the post-synaptic density (PSD) of neuronal cells. Related compositions include, but are not limited to, compounds that affect, positively or negatively, ADDL binding to neuronal cells, either via one or more receptors localized at the post-synaptic density (PSD) or otherwise. Related methods include, but are not limited to, procedures to screen for compounds that affect, either positively or negatively, ADDL binding to neuronal cells, either via one or more receptors localized at the post-synaptic density (PSD) or otherwise. Other related methods include, but are not limited to, prevention and treatment of ADDL-related diseases, such as Alzheimer's disease, mild cognitive impairment, Down's syndrome, and the like, using compositions that inhibit, block, or otherwise interfere with ADDL binding to one or more receptors localized at the post-synaptic density of neuronal cells.
EP0989973B1 Chalcones having antiproliferative activity Disclosed are compounds having general formula (A) wherein Ar représents phenyl, which may be unsubstituted or substituted by one, two or three substituents independently selected from Cl, Br, F, -OMe, NO2, CF3, C1-4 lower alkyl, -NMe2, -NEt2, -SCH3, -NHCOCH3; 2-thienyl; 2-furyl; 3-pyridyl; 4-pyridyl or 3-indolyl, and R represents -OCH2R1, in which R1 is selected from -CH=CMe2, -CMe=CH2, -C CH; with the proviso that where Ar represents phenyl, R is other than 3-methyl-2-butenyl. The compounds possess a valuable antiproliferation activity both on sensitive cancerous cells and on cells which are resistant to common chemotherapeutic drugs.
CN102188436A Injection for treating porcine mixed infection The invention discloses injection for treating porcine mixed infection. Each 100 liters of injection contains 10 to 15 kilograms of sulfamonomethoxine sodium, 2 to 5 kilograms of ofloxacin, 2 to 4 kilograms of diclofenac sodium, 1 to 2 kilograms of baicalin, 2 to 4 kilograms of trimethoprim, 0.1 to 0.2 kilogram of dexamethasone sodium phosphate, 0.1 to 0.2 kilogram of sodium thiosulfate, 3 to 6 liters of ethanolamine, 3 to 6 liters of phenyl carbinol, 30 to 60 liters of propylene glycol and the balance of water for injection. Compared with the conventional compound preparation for treating the porcine mixed infection, the injection effectively treats the porcine mixed infection and is convenient to use.
WO2008039023A1 Heteroaryl-pyrazole derivatives as cannabinoid cb1 receptor antagonists A heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing the inventive heteroaryl-pyrasole compounds or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
EP1333828B1 Prevention of development of dyskinesias The present invention relates to the prevention of the development of sensitization caused by chronic use of dopaminergic agents using an alfa2-adrenoceptor antagonist or a pharmaceutically acceptable ester or salt thereof.
CN101164550A Application of realgar microorganism leaching liquid in preparing antibiotic and antiviral medicine The present invention relates to an application of realgar microbial extract in preparation of medicine for resisting bacteria and resisting various. The realgar microbial extract is prepared according to the microbial treatment method disclosed by Chinese invention patent application 20061002000675. In the lowest arsenic concentration range (microgram grade) said extract has obvious effect for inhibiting colibacillus, staphylococcus aureus, candida albicans, bacillus subtilis, epidermal drug-resistant staphylococcus, comprodeum bacillus, non-drug-resistant epidermal staphylococcus, waxy epidermal staphylococcus, aeruginose pseudomonads and herpesvirus, etc. so that it can be used for preparing medicine for resisting bacteria and resisting virus., and can be made into various dosage forms, including suppository, pill preparation, granules preparation, film preparation, microcapsule preparation, dipping pills preparation, aerosol, tincture preparation, syrup, oral liquor and injection, etc.
US20120046291 Extended Triterpene Derivatives The present invention concerns novel pharmaceutically active triterpene derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (HIV).
WO2012135112A2 Methods for preparing deuterated 1,2,3-triazoles This disclosure relates to a method that involves reacting an azide with an alkyne in the presence of deuterated water and a copper-containing catalyst, thereby forming a deuterated 1,2,3-triazole.
EP2454263A1 3-hydroxypyrrolidine inhibitors of 5'-methylthioadenosine phosphorylase and nucleosidase The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (I) which are inhibitors of 5'-methylthioadenosine phosphorylase or 5'-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5'-methylthioadenosine phosphorylase or 5'-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.
US8232318 Approaches to treat cancer using HB-EGF inhibitors The invention provides methods for the treatment of cancer in a subject by the administration of myrsinoic acid A and/or one or more myrsinoic acid A analogs.
US20110268783 Partially microcellular, selectively hydrophilic composite construct for ocular drug delivery A partially microcellular, selectively hydrophilic composite as a self-standing construct or a component of a device for ocular delivery of at least one bioactive agent, the composite comprising a highly hydrophilic microcellular foam adjoined with a flexible hydrophobic barrier polymeric film.
WO2014075583A1 Stable oral solid drug composition of abiraterone and preparation method therefor A stable oral solid drug composition of abiraterone comprises abiraterone acetate and citrate which serves as a pharmaceutical adjuvant, wherein the weight ratio of citrate to abiraterone acetate is 1:100 to 1:5.
US7883707 Induction of antigen specific immunnologic tolerance Antigen specific immune tolerance is induced in a mammalian host by administration of a toleragen in combination with a regimen of immunosuppression. The methods optionally include a preceding conditioning period, where immunosuppressive agents are administered in the absence of the toleragen. After the tolerizing regimen, the host is withdrawn from the suppressive agents, but is able to maintain specific immune tolerance to the immunogenic epitopes present on the toleragen. Optimally, the toleragen will have high uptake properties that allow uptake in vivo at low concentrations in a wide variety of tolerizing cell types.
US20090023780 Therapeutic use of a derivative of thienylcyclohexylamine The invention concerns the use of a thienylcyclohexylamine, on its own or associated with other substances with pharmaceutical activity, for preparing a medicine designed to prevent and/or treat pain and/or nociception.
EP1816125A1 Novel crystalline forms of an antagonist of CB1 cannabinoid receptor and preparation method thereof The present invention relates to several crystalline forms and an amorphous form of an antagonist of CB1 cannabinoid receptor and methods for their preparation. The present invention is also directed towards pharmaceutical compositions comprising these polymorphs ofrimonabant. The invention provides method of treating obesity, smoking cessation, overweight and related diseases by administering to a patient in need thereof a therapeutically effective amount of the different polymorphic forms and the amorphous form of the current invention.
CN101732448A External quick-acting medicament for treating tumor and breast cancer and production process thereof The invention relates to an external quick-acting medicament for treating a tumor and a breast cancer and production process thereof. The medicament comprises the following raw material components in percentage by weight: 25 to 30 percent of peach twig extract dry powder, 40 to 50 percent of perilla leaf extract dry powder and 25 to 30 percent of oxalicacid crystal product extract dry powder. In addition, each 150g of medicament is mixed with 20 to 30g of clerodendrum bungei extract paste for diminishing inflammation of wounds and curing the wounds. The peach twig extract dry powder contains 1 to 1.6 percent of natural plant antibiotics with properties of alkaloid, and also contains amyrin, naringenin, persicoside, persicogenin and salipurposide; a perilla leaf extract comprises alpha-bergamotene, beta-caryophyllene, cumic acid, dihydro perillyl alcohol, isoegomaketone, l-limonene, linalool, menthol-b, 1.2methylenedioxy-4-methoxy-5-allyl-benzene-3-alkynyl-beta-D-glucopyranoside, perilla olefine aldehyde, and beta-sitosterol; and the oxalicacid crystal dry powder is water-soluble powder. The external quick-acting medicament has the effects of killing viral cells one time, calcifying lesion tissues and discharging focus out of body, and achieves obvious and quick effect of treating both tip and root.
CN101836958A Preparation of taxane pH sensitive nanoparticles composite for oral administration and application thereof The invention relates to a preparation of taxane pH sensitive nanoparticles composite for oral administration and application thereof. The invention is characterized in that taxane medicine is enveloped in nanoparticles made of a pH sensitive high polymer material to prepare a nanometer dose administration system. The system can obviously improve the dissolution rate of slightly soluble medicine, has obvious pH sensitivity, and releases medicine at the particular position of intestinal tract, which is favorable to improving the bioavailability and local targeted performance of the medicine. The preparation has good application foreground in the tumour treatment, in particular to the local tumour treatment of gastrointestinal tract.
CA2513427C Compounds having anti-proliferative properties There is provided a method of inhibiting the occurrence of one of more of the following conditions: - the proliferation of monocytes/macrophages; or - the proliferation of smooth muscle cells; or - the expression of CD36 receptors; or - the uptake of oxidized LDL, the method comprising the step of administering an effective amount of one or more phosphate derivatives of one or more electron transfer agents.
US20110092568 Modulation of mlck-l expression and uses thereof In various aspects and embodiments the invention provides methods and reagents for controlling gene expression, and for treating disorders and diseases. Embodiments provide methods and reagents specifically for the regulation of MLCK expression and for the use thereof in treating disorders and diseases. Various embodiments provide methods and reagents for specifically down regulating the expression of MLCK-L more efficiently than that of MLCK-S, and for the use thereof in treating disorders and diseases. Embodiments provide siNA for the same, particularly siRNAs. Various of the embodiments are useful for the treatment of inflammatory disorders and diseases, including, for one example in the regard, Asthma.
WO2011049058A1 Water-based paste containing diclofenac sodium Provided is a water-based paste containing diclofenac sodium, which is obtained by mixing a uniform mixed solution of diclofenac sodium wherein the mixture ratio of crotamiton/diclofenac sodium is 8.0 or less and the mixture ratio of (water + crotamiton)/diclofenac sodium is within a range of 3.0 to 20.0.
EP2135871A1 New trinem antibiotics and inhibitors of beta-lactamases The present invention relates to a compound of formula (I) in particular compounds of formula (Ia), the use of a therapeutically effective amount of one or more compounds of formula (I) or (Ia) as a broad-spectrum antibiotic and the use of a pharmaceutical composition comprising said compounds for the treatment of bacterial infections in humans or animals.
WO2013149959A1 Salts of 5-[(1r)-2-({2-[4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1h)-one The present invention is directed to a pharmaceutically acceptable crystalline addition salt of (i) 5-[(1R)-2-({2-[4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.
CN1839812B Glibenclamide solid dispersion agent , oral single-ingredient or compound formulation and its preparation method The invention relates to a Glibenclamide solid dispersion prepared through solvent method, which comprises Glibenclamide 2-14 parts, carrying agent 4-28 parts, organic solvent 100-900 parts. The compound preparation provided by the invention contains 0.399-1.035mg of Glibenclamide solid dispersion, 250mg of metformin hydrochloride, and one or more pharmaceutically acceptable carrying agents.
WO2009064590A3 Therapeutic applications of p53 isoforms in regenerative medicine, aging and cancer The present invention provides methods and compositions for modulating cell senescence and cell proliferation using isoforms of the p53 tumor suppressor protein. The methods and compositions of the invention find use in inhibiting cancer cell growth or in generating populations of cells for tissue regeneration through the modulation of cell senescence and proliferation.
US8758826 Cannabinoid receptor binding agents, compositions, and methods A composition comprising a cannabinoid receptor binding agent attached to a particle for the treatment of skin conditions. The particle may be a nanoparticle, such as nanocrystalline cellulose. The particle may further be modified with functional moieties. Drug delivery properties may be modified by coating the particles or using vesicles to deliver the cannabinoid receptor binding agent and particle. A substrate may be used to deliver the composition to the skin.
CN102512381A Lansoprazole medicine composition used for injection The invention aims at providing a lansoprazole lyophilized medicine composition used for injection. According to the invention, lansoprazole is dissolved in a solution of sodium hydroxide and mannitol; the obtained solution is lyophilized, such that the medicine composition is obtained. In the medicine composition, a weight ratio of lansoprazole:mannitol:sodium hydroxide is 2-8.5:2-8.5:1, and preferably 6:6:1. The medicine composition is advantaged in simple formula and small amount of auxiliary materials. Therefore, side effects caused by excess dosages of auxiliary materials are overcome; a lyophilization time is greatly reduced, such that unnecessary energy consumption is saved. Therefore, the lansoprazole medicine composition has certain competitive strength in markets.
CA2790646A1 Silicon-containing biodegradable material for anti-inflammatory therapy The present invention relates to a silicon-containing biodegradable material for the prophylaxis and/or the treatment of diseases which are associated with an elevated interleukin-1ß and/or interleukin-6 and/or interleukin-8 activity and/or which can be treated by reducing such an activity or such cytokine activity.
CN1951367B Fat emulsion containing hydroxycamptothecine and preparation method thereof The invention relates to an intralipid containing hydroxycamptothecin and process for preparation, wherein the preparation mainly comprises (by weight percent) hydroxycamptothecin 0.001-0.04%, oil for injection 5-30%, emulsifying agent 1-9%, stabilizing agent 0.1-1%, solubilizing agent 0.5-8%, isotonic conditioning agent 2-3%, anti-oxidant 0.01-0.05% and balancing water for injection, the pH is adjusted to 5-7.
CN101485666B Application of Gamabufotalin and salt thereof in preparing medicament for treating gynaecologic tumor The invention provides application of gamabufotalin and a salt compound thereof in preparation of a medicine for treating gynecological tumor. By comparing in vitro anti-cancer experiments of a bufadienolide extract and monomeric compounds, namely the gamabufotalin, cinobufagin, bufalin and bufotalin as well as hydrochlorides or sulfates of the four compounds to four gynecological tumors, namely human ovarian cancer cells A2780, human ovarian cancer cells SK-OV-3, human cervical carcinoma cells and human endometrial cancer cells, an experimental result shows that the gamabufotalin has stronger activity against gynecological tumor cells than the bufadienolide extract and the monomeric compounds, namely the cinobufagin, the bufalin and the bufotalin, and the hydrochloride or the sulfate of the gamabufotalin has stronger activity against gynecological tumor cells than the hydrochlorides or the sulfates of three compounds, namely the cinobufagin, the bufalin and the bufotalin. The gamabufotalin and the salt compound thereof provided by the invention have the advantages of clear components, controllable quality, strong anti-cancer activity, and small adverse reaction, and are expect tobe developed into a novel anti-cancer drug.
CN101015565A Vaginal abluent A vagina rinsing agent for women relates to the field of health products for sterilization. The invention provides a vagina rinsing agent with remarkable sterilizing effect, low pungency, no interfferance to microenvironment, and good nutritive function and stability in order to solve the problems in present technology. the rinsing agent comprises (by mass unit) active components containing Iodine 1-10; cosolvent 0.6-8 selected from potassium iodide, sodium iodide, and ammonium iodide; carrier material 10-150 including alkylphenol polyoxyethylene such as nonyl, octyl, dodecyl, and tetradecyl; pH regulator 10-60 selected from one or more of amino acids or their salt; and water 20-978.
US20110021480 17-beta HSD1 and STS Inhibitors Substituted steroid compounds which represent selective inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17β-estradiol concentration.
WO2010054158A2 Steroid modulators of glucocorticoid receptor The present invention relates to new steroid modulators of glucocorticoid receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
US20120282245 Biomarkers and assays for the treatment of cancer This invention features methods for prognosticating the efficacy of a cancer treatment comprising administration of a lymphotoxin-β receptor (LT-β-R) using TRAF3, TRAF2, and/or p53 markers, as well as combination therapies that include a composition that activates lymphotoxin-beta receptor signaling in combination with one or more other agents.
WO2014056779A1 Drug for the prophylaxis and treatment of a neurodegenerative disease The invention relates to a drug for the prophylaxis and/or treatment of a neurodegenerative disease.
EP2601954A1 Therapeutic agent for disease A disease treatment drug having high pharmacological effects and no side effects is provided, the disease treatment drug being capable of intensively delivering an iron or manganese porphyrin complex capable of removing active oxygen to abnormal tissue within a living body, and effectively removing the active oxygen within the abnormal tissue. The disease treatment drug contains an iron or manganese porphyrin complex nanocapsule housing an iron or manganese porphyrin complex within a nanosized capsule. In the disease treatment drug, disease of abnormal tissue having a high concentration of active oxygen can be treated by the iron or manganese porphyrin complex delivered into the abnormal tissue as a result of the nanocapsule, without affecting normal tissue having a low concentration of active oxygen, and side effects can be suppressed.
CN102406543A Ceftazidime injection solution packaged by double-cavity bag and preparation method thereof The invention discloses a ceftazidime injection solution packaged by a double-cavity bag. The medicinal composition of the injection solution comprises the following raw materials: 0.5-3 parts by weight of ceftazidime in a powder cavity, and 4-11 parts by weight of glucose injection solution with 100 parts by volume of glucose or 0.8-1 part by weight of sodium chloride injection solution with 100 parts by volume of sodium chloride in a solution cavity. The ceftazidime injection solution is packaged by the double-cavity bag; the sterilized ceftazidime powder and the solvent (sodium chloride injection solution or glucose injection solution) are filled in two cavities separated by pseudo soldering separations respectively; and when the ceftazidime injection solution is used, pseudo soldering isolating bars can be connected by extruding a medicine bag only, and the sterilized ceftazidime powder and the solvent are quickly solved and mixed under the sealed and sterilized condition to form a total medicine treatment mixed solution which can be directly applied to the patient.
US20080119555 Aryl Alkyl Sulfonamides As Therapeutic Agents For The Treatment Of Bone Conditions The present invention pertains to certain aryl alkyl sulfonamides and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formula: wherein: Ar1 is independently C5-20aryl (e.g., biphenyl, phenanthryl, fluorenyl, or carbazolyl, most preferably biphenyl), and is optionally substituted; RN is independently —H, acyl, C5-20aryl-C1-7alkyl, C3-20heterocyclyl, or C1-7alkyl, and is optionally substituted; Ralk is a C2-10alkylene group, and is optionally substituted; and Q is independently —H or an organic group having from 1 to 30 atoms selected from carbon, nitrogen, oxygen, sulfur, phosphorus, fluorine, chlorine, bromine, and iodine (e.g., an oxy-type group, an amine-type group, etc.); and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit osteoclast survival, formation, and/or activity, and to inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, in the treatment of bone disorders such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease, and the like; and/or in the treatment of conditions associated with inflammation or activation of the immune system.
CN1718590A Poria cocos mycellium glucan sulphate derivative and its preparation method and use A sulfate derivative of glucosan is prepared from the mycelia of tuckahoe through extracting water-insoluble alpha-glucosan, suspending it in anhydrous N, N-dimethylformamide, adding pyridine and chlorosulfonic acid, reaction, coding, dissolving in distilled water, regulating pH=9-10, adding alcohol, and depositing. It can be used to prepare anticancer medicine and health-care product for improving immunity.
CN103656649A Famotidine inclusion compound and preparation method The invention provides a famotidine inclusion compound and a preparation method. The inclusion compound comprises famotidine and glyceryl behenate. The preparation method comprises the following steps: the glyceryl behenate is heated to 80 DEG C through water bath or steam, stirring and fusion are performed on the glyceryl behenate at the temperature of 80 DEG C; the famotidine, which is equal to the glyceryl behenate in weight, is added into the fused glyceryl behenate, stirring and mixing are performed for 25-35 minutes at the temperature of 80 DEG C or homogenizing is performed through a homogenizer; the mixture prepared through the step 2 is fed into a spray dryer for drying before cooling, so that the famotidine inclusion compound is obtained. The famotidine inclusion compound has the benefits as follows: because the glyceryl behenate has the characteristics of hydrophobicity, anti-oxidation, hydrolysis prevention and the like, and is used for famotidine inclusion, the water absorption capacity of the famotidine self is reduced, and the famotidine is separated from other substances in the compound, the stability of the drugs is enhanced, the drug therapeutic effect is maintained, the bitter taste of the famotidine is covered up, and the bad taste during taking is reduced.
CA2241825C New monofunctionalized edta, dtpa and ttha derivatives and their use in medical diagnosis and therapy The invention relates to new monofunctionalized ethylenediaminetetraacetic acid, diethylenetriaminepentaacetic acid and triethylenetetraaminehexaacetic acid derivatives, their production and their use for the production of pharmaceutical agents.
CN101518598A Tea oral tablet and preparation method thereof The invention discloses a tea oral tablet and a preparation method thereof. The tea oral tablet uses theaflavin and theine-removing tea polyphenol as main raw materials, and filling agent, flavouring agent, bonding agent and disintegrant are added into the main raw materials to prepare the oral tablet product. The product has the physiologic function of the theaflavin and the tea polyphenol, is favorable to the oxidation resistance of a human body to remove free radicals for keeping the function of the human body and is easy to take and convenient to carry.
CN103083322A Medicinal composition containing injection cefmenoxime hydrochloride and compound amino acid injection The invention relates to a medicinal composition containing injection cefmenoxime hydrochloride and a compound amino acid injection, and especially relates to a medicinal composition packaged in a combination manner and comprising injection cefmenoxime hydrochloride and the compound amino acid injection. When the medicinal composition is used, the injection cefmenoxime hydrochloride is added to the compound amino acid injection, and the medicinal composition is intravenously dripped for 30min-2h. Compared with a compatible mixture of the injection cefmenoxime hydrochloride and the compound amino acid injection, the combination packaged medicinal composition allows the steps to be simplifies, the safety to be improved, the stability of cefmenoxime hydrochloride to be large and the clinical application quality and the bioavailability of the medicinal composition to be improved.
US20100190823 Therapeutic ((Bicylicheteroaryl)Imidazolyl) Methylheteroaryl Compounds Disclosed herein is a compound of the formula (I) therapeutic methods, compositions, and medicaments related thereto are also disclosed.
CN101855234A Preparation of 6-oxa-8alpha-steroid estrogen analogues - a new group of unnatural estrogens and their use in medicine The invention is related to the area of new 6-Oxa-8a-steroid estrogen analogues and the synthesis of these new biological active steroid estrogen analogues, namely, to the preparation of 6-oxa-8a-steroid estrogens and their use as estrogen receptor modulators. These new estrogen analogues are ligands for estrogen receptors and as such may be useful for the treatment and prevention of a variety of conditions related to estrogen functioning. These conditions include bone and cartilage disorders, increased levels of LDL cholesterol, cardiovascular diseases, impairment of cognitive function, cerebral degeneration disorders, endometriosis and other types of inflammation, the metabolic syndrome, and cancer, in particular of the breast, uterus and prostate.
EP1228052B1 1-cyclic amino-alkylcyclohexane compounds, pharmaceutical compositions thereof, and their use as anticonvulsants Certain 1-cyclic amino-alkylcyclohexanes selected from the group consisting of those of formula (I) wherein R* is -(CH2)n-(CR6R7)m-NR8R9; wherein n+m=0,1, or 2; wherein R1 through R7 are independently selected from the group consisting of hydrogen and lower-alkyl (1-6c), at least R?1, R4, and R5¿ being lower-alkyl, and wherein R?8 and R9¿ together represent lower-alkylene -(CH¿2?)x- wherein x is 2 to 5, inclusive, and enantiomers, optical isomers, hydrates, and pharmaceutically acceptable salts thereof, are systemically active uncompetitive NMDA receptor antagonists and are therefore useful in the alleviation of conditions resulting from disturbances of glutamatergic transmission. More importantly, these compounds exhibit outstanding anticonvulsant and anti-seizure activity which is not shared by closely-related noncyclic amino compounds. Pharmaceutical compositions thereof and a method-of-treating conditions which are alleviated by the employment of the same, especially the alleviation of convulsions and seizures, and method for the preparation of the active 1-cyclic amino-alkylcyclohexane compounds involved and the manufacture of medicaments therefrom.
CA2688463A1 Process for the preparation of rizatriptan The present invention relates to a novel process for the preparation of rizatriptan and its pharmaceutically acceptable salts. It provides a novel process for the preparation of highly pure rizatriptan, which can be easily adopted for commercial production with a high degree of consistency in purity and yield. Subsequently the rizatriptan base preparedcan be converted into any suitable pharmaceutically acceptable salt, such as the oxalate, succinate or benzoate salt,for dosage form preparation. The present invention also provides a composition comprising rizatriptan useful for the manufacture of a medicament for the treatment or prevention of migraine.
US6927220 Bicyclic-substituted 4-amino-pyridopyrimidine derivatives The invention relates to 6- or 7-bicyclic-substituted 4-amino-subsituted pyridopyrimidines and to pharmaceutically acceptable salts, prodrugs and hydrates thereof. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating hyperproliferative disorders abnormal cell growth in a mammal by administering the compounds.
US20100227826 Stable Flavonoid Solutions A stable flavonoid solution comprising (i) at least one flavonoid or flavonoid derivative selected from the group consisting of luteolin, myricetin, baicalin, baicalein, silymarin and kushenol, (ii) a mixture of alkyl glycols of two to seven carbon atoms, (iii) a polyol ether and (iv) an antioxidant.
CN1943596A Medicine for eye for preventing and curing conjunctivitis and keratitis and its preparing method The invention provides a medicine for eye use for prevention and cure of conjunctivitis and keratitis and its preparation process. Said invention prepare eye medicine of bear gall powder and compound baicalin into liquid or semi-solid medicine for eye use by modern preparation medicine technique for treatment of eye disease mentioned hereinabove.
US20110039880 Aryl substituted sulfonamide compounds and their use as anticancer agents Aryl substituted sulfonamide compounds of formula (I): wherein bond, X, Y, R1, R2, R3, m, and n are defined herein. Also disclosed is a method for treating cancer with these compounds.
CN101352446A Compound and use for the treatment of benign prostatic hyperplasia and relative diseases The present invention relates to the use of 1-alpha-fluoro-25-hydroxy-16,23E-diene-26,27-bishomo-20-epi-cholecalciferol, or a pharmaceutically acceptable salt or ester thereof, for the manufacture of a medicament for the prevention and/or treatment of benign prostatic hyperplasia (BPH) and associated symptoms.
CN103239456A Pharmaceutical composition for easing pain and use thereof The invention relates to a pharmaceutical composition for easing pain. The pharmaceutical composition is prepared from the following components according to the volume ratio: 2% methylthioninium chloride injection, 0.5% bupivacaine hydrochloride injection, 2% lidocaine hydrochloride injection and water for injection, of which the ratio is 2:5:5:16. The pharmaceutical composition relieves pain after being applied to an anorectal postoperative incision, improves local blood circulation, benefits for wound concrescence, contributes to wound bleeding, and reduces secreta. The pharmaceutical composition does not generate systemic adverse reaction after an operation, local edema or necrosis by a clinical test, and has no influence on local granulation tissue growth and wound concrescence; the anus has no abnormity, can smoothly defecate after the wound is repaired, has no untoward effect after follow-up treatment, and is reliable in curative effect. The drug disclosed by the invention removes a local hot pain after methylenum coeruleum is injected, does not generate an anesthesia clearance, is fast to take effect, and takes effect after being injected 2-4 hours; the reversible nerve damage disappears after about 15 days in general; and the requirement of wound growth just can be met.
US20100190757 Combination preparation for oral contreaception and oral therapy of dysfunctional uterine bleeding containing estradiol valerate and dienogest and method of using same The multiphase combination preparation for oral therapy of dysfunctional uterine bleeding and for oral contraception contains a first phase consisting of 2 daily dosage units, each containing 3 mg of estradiol valerate or <3 mg of estradiol; a second phase consisting of a first group of 5 daily dosage units, each consisting of a combination of 2 mg of dienogest with 2 mg of estradiol valerate or <2 mg of estradiol, and a second group consisting of 17 daily dosage units, each consisting of a combination of 3 mg of dienogest with 2 mg of estradiol valerate or <2 mg of estradiol; a third phase consisting of 2 daily dosage units, each containing 1 mg of estradiol valerate or <1 mg of estradiol; and another phase consisting of 2 daily dosage units of a pharmaceutically harmless placebos.
CN103623412A Stable cefaclor tablet composition and preparation method thereof The invention discloses a cefaclor tablet pharmaceutical tablet composition which comprises cefaclor, lactose, microcrystalline cellulose, crosslinked povidone, diethylene glycol monoethyl ether, colloidal silicon dioxide and glyceryl behenate or sodium stearyl fumarate. The preparation method comprises the following steps: evenly mixing the cefaclor with the pharmaceutical auxiliary materials; adding the colloidal silicon dioxide into the diethylene glycol monoethyl ether, heating while stirring for melting, and cooling to obtain a solid mixture; screening, and evenly mixing the cefaclor auxiliary materials; granulating by a dry process; and after finishing the granules, adding the lubricant, evenly mixing, measuring the intermediate content, determining the tablet weight, tabletting and packaging. The invention provides a legal and reasonable cefaclor table composition and a preparation method thereof, thereby obtaining the cefaclor tablet which has the advantages of stabler and more controllable quality, higher bioavailability and simpler technique.
US8703106 Chlorine dioxide treatment for biological tissue Methods for administration of a substantially non-cytotoxic chlorine dioxide composition to whiten a tooth surface are provided. The method comprises contacting a surface of a tooth with an efficacious amount of a composition comprising chlorine dioxide to provide an efficacious amount of chlorine dioxide to the tooth surface, wherein the contacting step comprises one or more of: i) contacting the tooth surface iteratively with at least two, substantially contiguous applications of a substantially non-cytotoxic composition comprising chlorine dioxide; ii) irrigating the tooth surface using an irrigation device that delivers a substantially non-cytotoxic composition comprising chlorine dioxide, or iii) irrigating the tooth surface using an irrigation device that comprises a chlorine dioxide composition comprising a cytotoxic amount of oxy-chlorine anions; and an oxy-chlorine anion barrier, wherein the irrigation devices delivers a substantially oxy-chlorine anion free chlorine dioxide composition to the tooth surface.
WO2011158924A1 Inhibitor of expression of dominant allele Disclosed is a method for designing an RNAi molecule which permits the expression of a wild-type or desired allele and can selectively and effectively inhibit the expression of only a specific dominant allele. Also disclosed is an inhibitor of the expression of a dominant allele containing the RNAi as an active ingredient. The inhibitor of the expression of a dominant allele contains an RNAi molecule having a structure in which a base length from a base point where a dominant point mutation occurs in a target dominant allele to the 5' end is set to a predetermined length and one mismatched base different from that in the sequence of a target gene is introduced at a predetermined position downstream of the base point.
US20080187572 Administering compound which stabilizes cadherin The present invention provides novel methods and compositions for the treatment and/or prevention of cataracts. A composition that inhibits destabilization of E-cadherin is administered. Preferably the composition comprises a matrix metalloproteinase inhibitor.
US20110182867 Modulation of bcl11a for treatment of hemoglobinopathies The invention relates to methods and uses of modulating fetal hemoglobin expression (HbF) in a hematopoietic progenitor cells via inhibitors of BCL11A expression or activity, such as RNAi and antibodies.
CN102133216A Combined medicine for curing treatment-resistant depression and applications thereof The invention relates to a combined medicine for curing treatment-resistant depression (TRD), which is characterized in that the combined medicine comprises paroxetine and sodium valproate. The invention also provides applications of the combined medicine. The invention has the advantages that the research on the TRD synergia strategy is provided for the first time in China, the combined medicine of paroxetine and sodium valproate, and the applications of the combined medicine in the preparation of medicine for curing the TRD are provided for the first time, the paroxetine combined with the sodium valproate for curing the TRD has higher remission rate, and the tolerance is high, so that the combined medicine can be taken as the new intensive treatment scheme for curing the TRD.
CA2369895C High affinity inhibitors for target validation and uses thereof This invention provides general methods for discovering mutant inhibitors for any class of enzymes as well as the specific inhibitors so identified. More specifically, this invention provides general methods for discovering specific inhibitors for multi-substrate enzymes. Examples of such multi--substrate enzymes include, but are not limited to, kinases and transferases. The mutant inhibitors identified by the methods of this invention can be used to highly selectively disrupt cell functions such as oncogenic transformation. In one particular example, this invention provides an Src protein kinase inhibitor, pharmaceutical compositions thereof and methods of disrupting transformation in a ceil that expresses the target v-scr comprising contacting the cell with the protein kinase inhibitor.
WO2004078140A3 SOLUBLE HYALURONIDASE GLYCOPROTEIN (sHASEGP), PROCESS FOR PREPARING THE SAME, USES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEREOF The invention relates to the discovery of novel soluble neutral active Hyaluronidase Glycoproteins (sHASEGP's), methods of manufacture, and their use to facilitate administration of other molecules or to alleviate glycosaminoglycan associated pathologies. Minimally active polypeptide domains of the soluble, neutral active sHASEGP domains are described that include asparagine-linked sugar moieties required for a functional neutral active hyaluronidase domain. Included are modified aminoterminal leader peptides that enhance secretion of sHASEGP. The invention further comprises sialated and pegylated forms of a recombinant sHASEGP to enhance stability and serum pharmacokinetics over naturally occurring slaughterhouse enzymes. Further described are suitable formulations of a substantially purified recombinant sHASEGP glycoprotein derived from a eukaryotic cell that generate the proper glycosylation required for its optimal activity.
US20100249211 N-Substituted-Aminomethylene Bridged Bicyclic Nucleic Acid Analogs Provided herein are bicyeMc nucleosides comprising a substituted amino group in the bridge, oligomeric compounds having at least one of these bicyclic nucleosides and methods of using the oligomeric compounds. The bicyclic nucleosides comprising a substituted amino group in the bridge are useful for enhancing properties of oligomeric compounds including nuclease resistance, in certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
WO2014008118A3 Method for concurrent treatment of pain and depression Provided herein are methods for the concurrent treatment of pain and depression in a patient based, at least in part, on the discovery that the comorbid interaction between pain and depression can be treated by regulating two opposing pathways of tryptophan metabolism.
CN1839807A Solution for disinfection and feet-protection Disclosed is a sterilizing food care liquid for treating skin diseases caused by fungus and various bacteria, wherein the percentage by weight of the ingredients include, DP300 0.2-0.5%, alcohol 15-25%, methyl glycol 55-70%, glycerin 2.5-4%, gourmet powder 0.5-1.5%, and distilled water 10-20%. The invention also discloses the process for its preparation.
WO2008053982A1 Composition for treating allergy The invention mainly belongs to the field of an ophthalmic pharmaceutical composition. Specifically, the invention provides a composition for treating an allergy characterized by adopting 3-hydroxybutyric acid used as a component in a conventional intraocular perfusate, therapeutic agent for corneal epithelium disorder or the like, particularly D-3-hydroxybutyric acid and/or a salt thereof as an active ingredient for treating allergic symptoms of the eyes or the like. By administering such a composition containing D-3-hydroxybutyric acid to the eyes of a rat, effects of suppressing itching of the eyes, suppressing eosinophilic infiltrationin the conjunctiva, suppressing conjunctivitis symptoms, increasing conjunctival microvascular permeability and the like were exhibited, therefore, it was shown that the composition is useful for improving the respective allergic symptoms. Further, D-3-hydroxybutyric acid is a biogenic substance, therefore, the composition of the invention is safe.
CN101088562A Anticancer composition containing ranimustine The anticancer composition includes effective anticancer component selected from tyrosine kinase inhibitor and/or ranimustine and slow releasing supplementary material, and may be prepared into slow released injection and slow released implant. The slow released injection includes also suspending agent and special solvent. The suspending agent has viscosity at 20-30 deg.c of 100-3000 cp and is selected from sodium carboxymethyl cellulose, etc. The slow releasing supplementary material is selected from p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP/TC), p(BHET-EOP/TC), p(BHDPT-EOP/TC), p(BHDPT-EOP/TC), p(CHDM-HOP), p(CHDM-EOP), etc. The released injection and slow released implant may be injected or set in tumor for slow releasing to maintain high medicine concentration for over 60 days to raise the treating effect and lower the systemic reaction on the medicine.
EP1676581A2 Polymer compositions for use in therapy The present invention relates to compositions for use in therapy, e.g. in phosphate-binding polymers which are provided for removing phosphate from the gastrointestinal tract. The polymers are orally administered, and are useful for the treatment of hyperphosphatemia.
US20090060898 Immune regulatory oligonucleotide (IRO) compounds to modulate toll-like receptor based immune response The invention provides novel immune regulatory oligonucleotides (IRO) as antagonist of TLRs and methods of use thereof. These IROs have unique sequences that inhibit or suppress TLR-mediated signaling in response to a TLR ligand or TLR agonist. The methods may have use in the prevention and treatment of cancer, an autoimmune disorder, airway inflammation, inflammatory disorders, infectious disease, skin disorders, allergy, asthma or a disease caused by a pathogen.
WO2013177672A1 Pharmaceutical composition of entecavir and process of manufacturing The present invention relates to an adhesive-free pharmaceutical composition for the treatment of hepatitis B virus infections, comprising at least one guanine-based antiviral active pharmaceutical ingredient. More specifically, the present invention concerns an oral pharmaceutical composition comprising: adhesive-free granules comprising therapeutically effective amount of entecavir and at least one intra-granular pharmaceutically acceptable excipient; at least one extra-granular pharmaceutical excipient, and, optionally, a moisture barrier coating. A method of manufacturing an adhesive-free pharmaceutical composition is also disclosed.
US7304053 Glycoprotein-mediated MDR Substituted heterocyclic compounds for treating multidrug resistance are disclosed. Compositions and methods of use for the substituted heterocyclic compounds are disclosed. Suitable substituted heterocyclic compounds include:
US7244755 Hydroxypropylamines Disclosed are compounds of formula I: and the pharmaceutically acceptable salts thereof wherein the variables RN, R1, R2, R3, RP and RC are defined herein. These compounds are useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
US20100196305 Sulfone polymer compositions Sulfone-containing copolymers and copolymer networks and compositions including sulfone-containing copolymers and copolymer networks may be used to bind target ions, such as phosphorous-containing compounds in the gastrointestinal tract of animals. In some cases, sulfone-containing copolymers and copolymer networks may be derived from a multi-amine monomer and a multifunctional sulfonyl-containing monomer comprising two or more amine-reactive groups.
CN1636599A Medicine composition and kit for local narcosis or relieving pain The present invention is medicine composition and kit for local narcosis or relieving pain of nervous tissue, especially dental pulp, of mammal. The medicine composition and kit includes one kind of local anesthetic, especially tetracaine, and one kind of compound capable of combining with SS1 and SS2 subunit of sodium ion channel.
US8158624 Purine PI3K inhibitor compounds and methods of use Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
WO2012102366A1 Method for producing novel piperazine compound Provided is a method capable of efficiently producing, with superior safety and superior industrial adaptability, a piperazine compound which has an anti-HCV action and which is useful as a therapeutic agent for hepatitis C. A method for producing a compound represented by structural formula (XIX) or a salt thereof, comprises a step for reacting a compound represented by structural formula (XVI) or a salt thereof with a compound represented by structural formula (XVIII) or a salt thereof (in the formulae, each symbol is as defined in the description).
CN103169689A Carvedilol transdermal controlled-release preparation for treating liver cirrhosis or liver fibrosis The invention relates to a preparation method, a formula, a drug release characteristic and pharmacological activity of a carvedilol transdermal controlled-release preparation for treating liver cirrhosis or liver fibrosis. The carvedilol transdermal controlled-release preparation can be used for treating the diseases related to liver cirrhosis or liver fibrosis. The invention relates to the preparation of various semi-solid and liquid transdermal controlled-release preparations or dosage forms such as patch, cream, gel and salve, or other semi-solid preparations, suspension, emulsion or other liquid preparations. According to the invention, the preparation provided by the invention is used for treating, improving and preventing the liver cirrhosis or liver fibrosis and the diseases related to liver cirrhosis or liver fibrosis by use of the controlled-release or slow-release characteristic of the carvedilol transdermal preparation, and can be independently used or combined with other medicines for treating liver cirrhosis or liver fibrosis.
DE102009034130A1 Aqueous pharmaceutical preparation, useful for the prevention of renal failure, comprises an aminoglycoside antibiotic, gelatin and/or its derivatives and/or a gelatin-like protein or polypeptide and sodium chloride Aqueous pharmaceutical preparation (I) comprises: 1-15 mg/ml of at least one aminoglycoside antibiotic; 20-100 mg/ml of gelatin and/or its derivatives and/or a gelatin-like protein or polypeptide; and up to 10 mg/ml of sodium chloride. An independent claim is included for a kit comprising at least a portion that contains aminoglycoside antibiotic and at least one further portion comprising a formulation of gelatin and/or its derivatives and/or a gelatin-like protein or polypeptide and sodium chloride. - ACTIVITY : Nephrotropic. - MECHANISM OF ACTION : None given.
US7105575 Methods for the treatment of neuro- disorders using aminothiol compounds The present invention relates to new uses of S-2-(3-aminopropylamino)ethyl dihydrogen phosphorothioate, (amifostine) and other aminothiol compounds to treat and reverse toxicities caused by therapeutic agents, radiation treatment or diabetes. In particular, the invention provides a method for treating neurotoxicity and nephrotoxicity associated with the administration of chemotherapeutic agents.
WO2013168131A1 Intrathecal administration of mtor inhibitors for the therapy of neurodegenerative, neuroinflammatory and neurooncologic diseases The invention relates to the use of inhibitors of the enzyme mTOR kinase (mammalian target of rapamycin) in the treatment of neuro-oncologic diseases, in particular tuberous sclerosis, neurodegenerative diseases, in particular Alzheimer's disease, and neuroinflammatory diseases, in particular multiple sclerosis and primary progressive aphasia, via intrathecal, or preferably intraventricular, administration of said inhibitors.
US20090170799 Modulation of c-reactive protein expression Compounds, compositions and methods are provided for modulating the expression of C-reactive protein. The compositions comprise oligonucleotides, targeted to nucleic acid encoding C-reactive protein. Methods of using these compounds for modulation of C-reactive protein expression and for diagnosis and treatment of disease associated with expression of C-reactive protein are provided.
US20090170895 S1p3 receptor antagonist The present invention relates to a medicine, and more particularly to novel arylamidrazone derivatives having an antagonistic action against S1P3 receptors and a medicine containing thereof as an active ingredient. The present invention provides an arylamidrazone derivative represented by the following formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents a C2-C8 alkyl group which may be substituted, a phenyl group which may be substituted, an aromatic heterocyclic group which may be substituted, a C2-C8 alkoxy group which may be substituted, or —NR4R5 (wherein R4 and R5, which are identical or different, each represent a hydrogen atom or a lower alkyl group which may be substituted, or R4 and R5 may be joined with the adjacent nitrogen atom to form a nitrogen-containing heterocyclic ring which may be substituted); R2 and R3, which are identical or different, each represent a hydrogen atom, a halogen atom, a halo-lower alkyl group, a lower alkyl group, a lower alkynyl group, a lower alkoxy group, a cyano group, a lower alkanoyl group or a lower alkylsulfonyl group; A represents a benzene ring or a heterocyclic ring; D represents a single bond or methylene; m represents an integer from 1 to 3, and n represents an integer from 1 to 5 (with the proviso that the case where R1 is an ethoxy group, R2 is a 2,4-dichloro group, R3 is a hydrogen atom, A is a benzene ring, and D is methylene; and the case where R1 is an ethoxy group, R2 is a 2,4-dichloro group, R3 is a hydrogen atom, a 2-methyl group, a 4-methyl group, a 4-methoxy group or a 4-ethoxy group, A is a benzene ring, and D is a single bond, are excluded).
EP1719779A2 Antibodies against Matin Antibodies to a protein with anti-angiogenic properties are disclosed and can be used for various therapeutic, diagnostic and prognostic applications.
CN103690698A Broad-spectrum antibacterial cream The invention discloses a broad-spectrum antibacterial cream. The broad-spectrum antibacterial cream is prepared from the following raw materials by weight: 0.1 to 0.3 part of Chinese angelica, 0.2 to 0.3 part of Chinese gall, 0.1 to 0.2 part of frankincense, 0.06 to 0.1 part of Chinese paris rhizome, 0.1 to 0.2 part of autumn zephyrlily herb, 0.1 to 0.2 part of bighead atractylodes rhizome, 0.1 to 0.2 part of dandelion, 0.4 to 0.6 part of Zornia gibbosa, 0.1 to 0.2 part of natural indigo, 0.2 to 0.5 part of myrrh, 10 to 14 parts of enoxacin, 45 to 55 parts of albolene, 18 to 25 parts of liquid paraffin, 75 to 85 parts of glycerin, 6 to 8 parts of sodium dodecyl sulfate, 0.8 to 2 parts of ethylparaben, 20 to 30 parts of cetanol, 40 to 55 parts of octadecanol and 700 to 800 parts of purified water. The cream provided by the invention has a broad-spectrum antibacterial effect, especially has high antibacterial activity on aerobic Gram-negative bacilli and exerts a good antibacterial effect on bacteria described in the specification in vitro.
CA2132544C Angiotensin ii antagonists against disorders associated with impaired neuronal conduction velocity, especially diabetic neuropathy This invention relates to the use of angiotensin II antagonists in treating or preventing the development of disease conditions associated with impaired neuronal conduction velocity, such as diabetic neuropathy, as well as their use in the manufacture of a medicament for use in such treatment. The invention also concerns pharmaceutical compositions containing an angiotensin II antagonist together with one or more other agents known to be of value in treating or preventing the development of disease conditions associated with impaired neuronal conduction velocity.
EP2572704A1 Orally-Disintegrating Formulations of Vildagliptin The present invention relates to an orally-disintegrating pharmaceutical tablet formulation, which is characterized by comprising vildagliptin or a pharmaceutically acceptable salt of vildagliptin and a coating which is selected from methyl methacrylate - diethyl aminoethyl methacrylate copolymer, polyvinylpyrrolidone having 3.5 - 5.5 mPa s or 5.5 - 8.5 mPa s viscosity, hydroxypropyl methyl cellulose having 3.5 - 5.5 mPa s viscosity.
US7371819 Differs from nucleotide sequence of wild-type IFN alpha -17 gene, in that it comprises one or several SNPs (Single Nucleotide Polymorphism[s]); anticarcinogenic and antiproliferative agents; side effect reduction The present invention relates to new polynucleotides derived from the nucleotide sequence of the IFNα-17 gene comprising new SNPs, and new polypeptides derived from the natural wild-type IFNα-17 protein comprising at least one mutation caused by at least one SNP of the invention, as well as their therapeutic uses.
CN101869687B Medicament for treating fatty liver and alcohol liver, and reducing blood lipid and aminotransferase The invention relates to a medicament for treating liver diseases and reducing blood lipid, in particular to a medicament for treating fatty liver and alcohol liver, and reducing blood lipid and aminotransferase, and solves the problem of treating the fatty liver and alcohol liver. The medicament is prepared from the following raw materials: Chinese caterpillar fungus, ginseng, hawthorn, kudzu-vine root, turmeric, liquoric root, cassia seed, Chinese magnoliavine fruit, oriental waterplantain rhizome, tea polyphenols, glycine, arginine, vitamin E, folic acid and zinc. The results of the animalexperiments and human clinical experiments show that the medicament of the invention has excellent effects of treating and preventing fatty liver.
WO2010075611A1 Composition comprising proanthocyanidin, proteolytic enzyme and aloe vera/agave species substance A composition comprising a proanthocyanidin, a proteolytic enzyme and a substance derived from Aloe Vera and/or from a plant of the Agave species, the composition being free of papain. Use of the composition for improving athletic performance, for improving health and wellbeing, for use as a sports isotonic drink or for the treatment of a condition selected from multiple sclerosis, cancer, diabetes, hypercholesterolemia, asthma, heart disease, liver disease and kidney disease.
WO2014138979A1 Pyrazole derivatives and their uses thereof The present disclosure relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein U, R1, R2, R3 and Q are as defined herein. The disclosure also provides a method for treating or preventing a method for the prevention, treatment and/or alleviation of one or more autoimmune or alloimmune disease, pharmaceutical compositions and combination comprising a therapeutically effective amount of a compound, as defined herein.
CN101744984A Formula for treating cough The invention relates to a formula for treating cough, which is composed of the raw materials by weight proportion: 10-15g of bulbus fritilariae, 15-20g of liquorice, 20-30g of pear slice, 5-10g of borneol, 3-5g of balloonflower root, 5-8g of radix bupleuri, 3-5g of fuodia rutaecarpa, 4-7g of almond, 10-25g of folia artemisiae argyi and 10-20g of honey. The formula has the advantages of significant treatment effect, short treatment period, small side effect and acceptable taste.
US20110020475 Cardioplegic solution The present invention relates to a new cardioplegic solution to arrest and protect the heart muscle during surgery. The cardioplegic solution according to the invention offers several significant advantages as compared to standard available solutions, and contains magnesium sulfate heptahydrate, potassium chloride, procaine hydrochloride and xylitol.
US20120040964 N-substituted piperidines and their use as pharmaceuticals The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
CN103524409A Quinoline compound as well as preparation method and application thereof The invention relates to the technical field of medicine, in particular to a quinoline tyrosine kinase inhibitor as well as a preparation and an application of the quinoline tyrosine kinase inhibitor in preparation of antineoplastic drugs. The structure formula (I) of a compound is as follows: the compound has good tyrosine kinase inhibitory activity, particularly, VEGFR2 and VEGFR3 inhibitory activities, and partial compound is subjected to liver microsome metabolic rate study, absorption characteristic study in a Caco-2 model and drug metabolism kinetic study.
WO2007119684A1 Spraying agent Disclosed is a spraying agent for spraying into the air. The spraying agent comprises a solution of γ-aminobutyric acid (as a solute) dissolved in a solvent.
CN103694254A Butene lactone compound containing sulfonyl lactones as well as synthesis method and application thereof The invention discloses a butene lactone compound containing sulfonyl lactones as well as a synthesis method and an application thereof, and belongs to the chemical field of medicines. The butene lactone compound has the following general structure formula I, wherein in the formula I, R represents hydrogen, mono-substituted or poly-substituted methoxy groups, methyl groups, fluorine, chlorine, bromine, trifluoromethyl and the like; the poly-substituted groups are same. The butene lactone compound has a good function of inhibiting HCV (Hepatitis C Virus) and cannot generate the significant cytotoxicity. Thus, the butene lactone compound can be used for preparing HCV-resisting medicines, and has the potential for developing the HCV-resisting medicines with novel functional actions.
WO2013120896A1 Compound for use in the prevention and/or treatment of a neurogenerative disease or a disease involving an activation of phosphodiesterase-4 (pde4) The present invention relates to a compound for use in the prevention and/or treatment of a disease selected from a neurodegenerative disease, especially Alzheimer disease, and a disease, disorder or condition involving an activation of phosphodiesterase-4 (PDE4), wherein said compound is of general formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X and Z each independently represent CH or N; Y represents O or S; R1, R2 and R3 may be the same or different and represent a hydrogen atom, a halogen atom, hydroxyl, nitro, cyano, amino, amido, carbamate, alkyl, alkenyl, alkynyl, alkoxy, heterocyclic, carbocyclic, alkylthio, carboxy, or alkoxycarbonyl; R4 represent a hydrogen atom; R5, R6, R7 and R8 may be the same or different and represent a hydrogen atom, halogen atom, hydroxyl, nitro, amino, alkyl, alkoxy, alkylthio, or tnfluoromethyl; R9 and R10 may be the same or different and represent a hydrogen atom, alkyl, alkylcarbonyl, heterocyclic, carbocyclic, ON02, or OS02R wherein R is hydroxyl, alkyl, carbocyclic; and R11 represents an alkyl, alkenyl, alkynyl, alkoxy, akoxycarbonyl, amino, amido, heterocyclic, carbocyclic, or optionally substituted azolyl.
CN101020010A Oral liquid for treating common cold heat The oral liquid for treating common cold and fever is prepared with giantreed root, sweet wormwood, bupleurum root, gypsum, polysorbate-80, sorbic acid and sweet essence in certain weight proportion. The preparation process includes decocting the first mentioned four materials, extracting volatile oil, merging and concentrating the decoction, filtering, and merging the decoction with the volatile oil and the other ingredients.
WO2009079878A1 Injection comprising docetaxel and its preparation The invention provides an injection comprising docetaxel, which contains a mother liquid, ethanol for preventing gel formation of injection, water for keeping the mother liquid in a uniformly flowing state. The mother liquid is a solution containing docetaxel and one or more pharmaceutically acceptable surfactants. The invention also provides a process for preparing the injection consisting of mixing the mother liquid with ethanol, then adding water and mixing uniformly. The injection has high uniformity and high stability, and can extend the time needed to form a crystal precipitation of docetaxel in the injectable solution.
CN101032544A Medicine composition of compound honeysuckle organic acid and the preparing method of the agent thereof The present invention discloses one kind of honeysuckle organic acid medicine composition and its preparation process, and features that the medicine composition consists of the effective parts, including honeysuckle organic acid, baicalin and houttuynine sodium. Scientific quality control method and dissolution measurement method have been established. The present invention determines the medicine material proportion and dosage through serial medicine efficacy screen experiments, the excipient and preparation process through dissolution experiments, and the high pharmacological effect of the preparations through pharmacological experiments.
US20100048551 Tricyclic Compounds Useful as Inhibitors of Kinases The present invention provides inhibitors of kinases, specifically IκB kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-κB-mediated diseases.
EP2183233A1 Dithiazolidine and thiazolidine derivatives as anticancer agents There is provided a compound of formula (I): wherein Y has the meaning given in the description. Such compounds are potentially useful in the treatment of disorders or conditions caused by, linked to, or contributed to by, excess adiposity, such as hyperinsulinemia and type 2 diabetes.
CN103462913A Galenic formulations of organic compounds The present invention relates to a solid oral dosage form comprising a therapeutically effective amount of aliskiren or a pharmaceutically acceptable salt thereof, and wherein the active incredient is present in an amount of more than 46% by weight based on the total weight of the oral dosage form.
CN103610670A Application of carmustin in preparation of medicine for treating lymjphoma The invention relates to an application of carmustin in preparation of medicine for treating lymjphoma. The animal experiments show that carmustin can kill large solid tumor in animal body, but also can induce the antineoplastic of the body for immunization. Carmustin can prevent cancer recurrence of cancer patient, which can not be achieved by other anticancer medicines. Research and development of carmustin have wide market prospect, and the carmustin can be effectively used for a lot of treatments of lymph cancer patients.
US7737118 Alternating intrathecal administration to the mammal of a pharmaceutically effective dose of opioid receptor agonist for first period of time, and dose of at least one opioid receptor-like receptor 1 agonist for a second period of time A method of producing analgesia in a mammal is provided by rotational (alternating) intrathecal administration to the mammal of a pharmaceutically effective dose of at least one opioid receptor agonist, such as a μ-, δ-, or κ-opioid receptor agonist for a first period of time, followed by intrathecal administration to the mammal of a pharmaceutically effective dose of at least one opioid receptor-like receptor 1 (ORL-1) agonist for a second period of time. The intrathecal drug administration of the first and second periods of time may be repeated a plurality of times without attaining tolerance in the mammal to either drug. Implantable apparatus for rotational administration of the active agents is also disclosed.
WO2008083367A2 Polycyclic heteroaryl substituted triazoles useful as axl inhibitors Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
WO2010088827A1 Novel uses of huperzine a and ophthalmic preparations thereof The uses of huperzine A in the preparation of medicaments for preventing or treating glaucoma, raised intraocular pressure, or ophthalmic diseases accompanied with impaired retinal ganglial cells, in-situ eye gels of huperzine A and eye drops of huperzine A for the same uses are disclosed. After a large number of cell and animal experiments, it is proved that huperzine A has good protective effect on retinal ganglial cells and the effect of lowering intraocular pressure after oral or transocular administration, thus can be used for preventing or treating glaucoma, raised intraocular pressure, or ophthalmic diseases accompanied with impaired retinal ganglial cells.
CN1615852A Indirubin oral dripping pill and preparing process The indirubin dripping pill containing indirubin 1-12 mg and proper amount of dripping pill medium in each pill. The dripping pill medium is one or two of polyglycol-6000, polyglycol-4000, polyoxyethylene monostearate, sodium stearate, glycerin, gelatin, poloxamer, stearic acid, glycerin monostearate and insect wax. The preparation process of the indirubin dripping pill includes melting and mixing indirubin and dripping pill medium, dropping at 60-120 deg.c into condensating agent, and eliminating condensating agent. The condensating agent is one or two of dimethyl silicon oil, liquid paraffin, tea seed oil and rape seed oil. The indirubin dripping pill is dark red. The indirubin dripping pill is used in treating chronic granulocyte leukaemia, and has the features of less side effect, low dosage, high medicinal effect, no obvious inhibition on marrow of patient, etc.
US20050159488 D-serine transport antagonist for treating psychosis Method and composition for augmenting NMDA receptor mediated neurotransmission involving use of a D-serine transport inhibitor.
US20110135577 Superparamagnetic nanoparticles IN MEDICAL THERAPEUTICS and manufacturing method THEREOF The successful transfer of therapeutic agents such as genetic materials (e.g. nucleic acid) or drug into living cells is the most important issue depending on the development of the delivery carrier. A method for manufacturing superparamagnetic nanoparticles in medical therapeutics is described to develop nano-sized calcium phosphate (CaP) mineral was rendered magnetic as delivery vehicle. The CaP-based magnetized nanoparticles (NPs) were possessed superparamagnetic property by hetero-epitaxial growth of magnetite on the CaP crystallites and also showed no harm to the cultured cells and elicited no cytotoxicity. The magnetized CaP was demonstrated to have good plasmid DNA binding affinity or drug carrying capacity. It significantly increased the expression of gene transfection and efficiency in delivery to mesenchymal stem cells (MSCs) under exogenous magnetic field. According to the above facts, this newly-synthesized magnetized CaP NPs has great potential as a novel non-viral targeted delivery vehicle to be applied for medical applications.
US20130316990 Use of vitamin d compounds Animal feed with 25-hydroxy vitamin D3 added, optionally in combination with vitamin D3, improves bone strength in animals, particularly pigs.
USRE42755 Honey based wound dressing The present invention is directed to the use of honey in medical dressings. Preferred embodiments modify honey with a viscosity increasing agent, resulting in a range of possible compositions including ointments and salves, self-adhesive gels such as for use on mouth ulcers and pustules, and pliable or flexible sheets which can be used as a wound covering. Preferred viscosity increasing agents include both particulate and continuous gels, respective examples of each including agars and alginates. Selected honeys preferably, but not necessarily, exhibit antibacterial properties other than what is merely conferred by osmolarity and sugar concentration effects.
WO2009100656A1 2-methylene-5-substituted methylene cyclopentanone derivatives and use thereof 2-methylene-5-substituted methylene cyclopentanone derivatives of formula I and use thereof. The derivatives of formula I as active components are used for preparing a medicine for curing and/or preventing a cancer disease, e.g. breast carcinoma, lung cancer, cancer of colon, rectum cancer, stomach cancer, carcinoma of prostate, bladder carcinoma, uterus cancer, pancreas cancer and ovary cancer. The active compound of the invention may be used as unique anticancer drug and may also be used in combination with one or more other antitumor drugs. Combined therapy is carried out by administrating each therapeutic component concurrently, subsequently or separately.
US6930118 3-Oxadiazol-5-yl-1-aminoalkyl-1h-indole derivatives The invention provides aminoalkylindole compounds of Formula (I), wherein R1-R5, n and p are as described. Also provided are compositions containing compounds of Formula (I) and the use of compounds of Formula (I) in modulating the activity of a cannabinoid receptor in a subject. In particular, the invention provides the use of such compounds as analgesic agents
CN101787015A Chiral tricyclic compounds with anti-histamine activity, preparation method and application The invention discloses chiral tricyclic compounds with anti-histamine activity, a preparation method and application. The chiral tricyclic compounds with the anti-histamine activity have a structural formula, wherein when R1 is phenyl or hydroxyalkyl, ester alkyl or carboxyalkyl of C1 to C11, R2 is straight-chain alkyl of C1 to C7; R3 is hydrogen or alkyl of C1 to C4; R4 is hydrogen or alkyl of C1 to C4; R5 is hydrogen or alkyl of C1 to C4; and R6 is hydrogen or alkyl of C1 to C4. Experiments prove that the chiral tricyclic compounds with the anti-histamine activity can be competitively combined with the body H1 receptor to block the action of the histamine and the H1 receptor so as to restrain the biological effect of the histamine and play a role in allergic resistance. The experiments show that the compounds have stronger anti-histamine activity compared with a positive contrast chlorpheniramine group.
CN102088954A An intrauterine delivery system for contraception The invention relates to a method for contraception and for reducing menstrual problems and inducing amenorrhea, wherein an intrauterine delivery device is used for the controlled release of a combination of progestogen or a drug having a progestogenic activity and at least one therapeutically active substance capable of preventing or suppressing abnormal and/or irregular endometrial bleeding over a prolonged period of time.
WO2006101407A1 Injection formulation containing the elements selenium and iodine A formulation for parenteral administration is described which includes: iodised oil, a selenium source such as barium selenate particles and a thickening agent such as beeswax. The formulation components ensure that the selenium source remains substantially suspended within an iodised oil mixture before and after administration. The formulation on administration forms a depot and slowly releases iodine and selenium over an extended time period of at least 90 days. The formulation has the advantage of providing a single dose product for delivery of both iodine and selenium elements to an animal such as a sheep and, has also been found to pass to progeny when administered to a ewe during gestation. Associated methods and uses are also described for administering the formulation and to manufacture the formulation. Further methods are also described to measure iodine levels and from the results determine whether or not iodine supplementation is required.
CN102058850A Application of medicine composition using oil of zedoary turmeric and borneol as raw materials The invention discloses novel application of a medicine composition using oil of zedoary turmeric and borneol as raw materials, belonging to the technical field of medicines. Researches on the pharmacodynamics tests and the clinical tests prove that the medicine prepared from the oil of zedoary turmeric and the borneol as raw materials is taken as the curative medicine, the medicine composition disclosed in the invention has excellent therapeutic action on constipation and better useful effect on the constipation.
WO2007109174A3 Compositions and methods for modulation of mcl-1 expression Disclosed herein are compounds, compositions and methods for modulating the expression of Mcl-1 in a cell, tissue or animal. Also provided are methods of target validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders.
US7932249 Olanzapine pamoate dihydrate The present invention relates olanzapine pamoate dihydrate, pharmaceutical compositions thereof and use in treating certain mental disorders, such as schizophrenia.
US20060040935 Method of treating impotence due to spinal cord injury A class of cGMP PDE inhibitors, including sidenafil and pharmaceutically acceptable salts thereof, which can be used to treat sexual dysfunction in male and female animals, especially humans, with a spinal cord injury. The invention can be used to treat sexual dysfunction in male animals that exhibit essentially no residual penile function.
US20100267799 Orodispersible pharmaceutical composition of perindopril The invention relates to a solid orodispersible pharmaceutical composition of perindopril, characterised in that it comprises perindopril or a pharmaceutically acceptable salt thereof and granules consisting of co-dried lactose and starch.
CN101564379A Methazolamide lipidosome and manufacture method thereof The invention provides a methazolamide lipidosome and a manufacture method thereof. The methazolamide lipidosome prepared by carrier materials, such as methazolamide, phospholipids, cholesterin, a surface active agent, and the like directly drips into the eyes to increase the density of medicines in the aqueous humor and prolong the detention time of the medicines in the eyes, has a certain action on glaucoma treatment and intraocular pressure reduction and has no obvious toxic side effect. The invention prepares 0.1 percent to 5 percent of methazolamide lipidosome solution for eye drop use, has simple and convenient preparation method and obvious pressure reduction effect and provides convenience for clinic application.
WO2009037398A2 Foodstuff composition to improve digestibility of foodstuff lipids The invention relates to human or animal food and more particularly to a food composition for improving digestibility of foodstuff lipids, comprising one or more lysophospholipids and/or phospholipids. The invention further relates to a foodstuff containing said food composition and a method for improving the digestibility of foodstuff lipids.
CN101199848A Drug compound for Ca channel retarder/diuretic/ folate coupling and function The invention relates to a drug combination of applying jointly calcium channel blocker/diuretic/folacin and the purpose. The combination includes: officinal dose of calcium channel blocker, officinal dose of diuretic, officinal does of folic acid compound and pharmacy-acceptable carrier. The invention provides the purpose of the combination in preparing the medicine used for preventing, treating or delaying hypertension, target organ damage caused by hypertension or hypertension-related diseases; the invention also provides the purpose of the drug combination in preparing the medicine used for reducing the danger of cardiovascular and cerebrovascular events caused by hypertension, in particular for reducing the incidence of cerebral apoplexy. The implementation of the invention, which provides the patient with the drug combination, can improve the curative effect, increase the compliance of the patient, convenience the drug administration and reduce the medical expenses.
US20100129468 Antifungal foam containing ciclopiroxolamine and zinc pyrithione and medical and cosmetic applications thereof The invention relates to a composition in the form of an emulsion that can be expanded by an aerosol dispenser, characterised in that it comprises from 15 to 20 volume % of alcohol, from 1 to 10 volume % of C3-C8 polyolen, a thickening agent, at least one non-ionic surfactant, a wetting agent, and one or more active ingredients dissolved or in suspension; the invention also relates to the medical and cosmetic applications thereof.
WO2007000464A1 Novel 3-aza-spiro[5.5]undec-8-ene derivatives and their use as monoamine neurotransmitter re-uptake inhibitors This invention relates to novel 3-aza-spiro[5.5]undec-8-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
CN101953860A Wet tissue for relieving hemorrhoid symptom and production method thereof The invention discloses a wet tissue for relieving hemorrhoid symptoms and a production method thereof, wherein the wet tissue is composed of a non-woven fabric as a carrier and a solution attached to the non-woven fabric. The invention is characterized in that the solution is prepared from the following raw materials in proportions: 2-3 percent of witch-hazel extracting solution, 1-1.5 percent of glycerol, 1-1.5 percent of propylene glycol, 0.5 percent of triclosan-II, 0.2 percent of IPBC-II and the balance of pure water. The invention has the effects of effectively relieving the hemorrhoid symptoms, protecting an affected part from being continuously damaged any more and effectively inhabiting the bacterial breeding so as to protect the skin.
CN103193792A New compound for treating ischemic cardiovascular and cerebrovascular diseases The invention provides a new compound shown in the formula I in the specification and a salt thereof. Experiments prove that the new compound can be used for treating and preventing cerebral ischemic diseases and improving sleep. The sodium salt of the new compound has good water solubility and can be used for preparing injection. Irritation tests show that the sodium salt has better tolerance and good safety.
WO2012159959A1 2-amino-3-(imidazol-2-yl)-pyridin-4-one derivatives and their use as vegf receptor kinase inhibitors The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.
WO2009037413A1 Dimers of 5- [ (4-cyanophenyl) sulfinyl] -6-methyl-2-oxo-1- [3- (trifluoromethyl)phenyl] -1,2-dihydropyridine-3-carboxamide as inhibitors of human neutrophil elastase for treating respiratory diseases Six specific compounds having human neutrophil elastase inhibitory activity are disclosed, one of which has the structural formula wherein A- is a pharmaceutically acceptable anion. The compounds are useful inter alia for the treatment of inflammatory respiratory disease, and may be administered by inhalation.
US7105483 Phosphinic pseudopeptide derivatives for the selective inhibition of the C-terminal active site of angiotensin I converting enzyme (ACE) The invention relates to the use of phosphinic pseudopeptide derivatives for production of a medicament for selectively inhibiting the active C-terminal site of angiotensin I converting enzyme. These derivatives are of formula (II): where, R1 may be a protecting group for amino functions usually used in peptide chemistry or an amino acid or a peptide protected by the above type of protecting groups, R2 and R3 correspond to a natural or unnatural amino acid side chain and R4 and R5 represent a hydrogen atom or a counterion.
CN102512369A Glycyrrhetinic acid solid lipid nanoparticles and preparation method for same The invention relates to glycyrrhetinic acid solid lipid nanoparticles and a preparation method for the same, belonging to the field of medicinal preparation. The main ingredients of the glycyrrhetinic acid solid lipid nanoparticles disclosed by the invention comprise active raw material glycyrrhetinic acid, medicinal phospholipid, a lipid material and a surfactant. The glycyrrhetinic acid solid lipid nanoparticle solution and the freeze-dried powder injection thereof prepared by the preparation method disclosed by the invention are small in particle diameter, high in entrapment efficiency, good in stability and capable of being used for a plurality of administration routes such as oral administration and injection administration. The glycyrrhetinic acid solid lipid nanoparticles disclosed by the invention can reduce dosage, enhance curative effect and reduce the toxic and side effects of medicine, as well as are suitable for treating a plurality of diseases such as hepatitis, liver cancer, lung cancer, ovarian cancer, gastritis, gastric cancer, leukaemia and aids.
US20120141488 Novel g protein coupled receptor protein and use thereof Disclosed are novel GPCR (G Protein Coupled Receptor) proteins and genes encoding the same. Also provided is the use of the proteins and the genes. Particularly, contemplated are a novel GPCR (G Protein Coupled Receptor) polypeptide, a polynucleotide coding for the same, a recombinant vector carrying the polynucleotide or a fragment thereof, host cells transformed with the vector, a transgenic animal infected with the vector. Also, a composition for detecting a cancer marker, comprising an agent capable of measuring the expression level of mRNA or protein of the GPCR polynucleotide, a kit for the diagnosis of cancer, comprising the composition, and a method for detecting the GPCR polypeptide and a gene encoding the polypeptide are provided. Further, a composition for the treatment and prevention of cancer, comprising an oligonucleotide inhibiting the expression of a gene encoding the GPCR polypeptide or an antibody against the GPCR protein, and a method for screening a modulator of the GPCR protein or a cancer therapeutic agent are provided.
CN102949593A Medicament for moistening lung and arresting cough The invention discloses a medicament for moistening the lung and arresting a cough. The medicament comprises the following raw materials in part by weight: 1-2 parts of large-leaved gentian, 2-4 parts of rhizoma polygonati, 2-3 parts of amber, 5-9 parts of adenophora verticillata, 3-5 parts of prepared radix rehmanniae, 1-4 parts of ophicalcitum, 2-4 parts of flos farfarae, 1-2 parts of poria peel, 2-5 parts of plantain herb, 3-6 parts of concha arcae, 1-4 parts of pseudostellaria, 1-3 parts of paniculate swallowwort root and 1-2 parts of mylabris radix asparag. The medicament for moistening the lung and arresting the cough not only has the functions of clearing heat, nourishing yin, moistening the lung, arresting the cough, tonifying qi, replenishing blood, promoting the secretion of saliva or body fluid and nourishing the spleen and the stomach, but also can dissolve phlegm, disperse blood stasis, soften hard lumps, dissipate stagnation, relieve hyperacidity, stop pain, calm the mind, induce urination, invigorate the circulation of blood and reinforce the kidney. The medicament is sweet and suitable for both the young and the elder.
US7034027 Method of treating a male or female animal in the treatment of a condition where inhibition of a cGMP-specific PDE is of a therapeutic benefit comprising treating said animal with an effective amount of a pharmaceutical composition with carriers Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
US20080306090 Thiourea derivatives Thiourea compounds of the following formula: wherein n, R1, R2, R3, A1, A2, X, Y, and Z are defined herein. Also disclosed is a method of treating hepatitis C virus infection with these compounds.
WO2007037685A1 Novel antibiotics comprising bis(1-aryl-5-tetraz0lyl)methane derivatives The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds, the bis(1-aryl-5-tetrazolyl)methanes, which are especially useful for combating infections with gram-positive bacteria and especially MRSA.
CN101485646B Andrographolide catablasm and preparation method thereof The invention relates to an andrographolidume cataplasm for transdermal administration and a method for preparing the same. The andrographolidume cataplasm consists of a backing layer, a medicine storehouse layer and a protective layer, wherein the medicine storehouse layer consists of hydrophilic substrate and a medicine; the hydrophilic substrate comprises the following components in proportion: 0.1 to 0.5g of polyvinyl alcohol, 1 to 3ml of glycerin, 1 to 5ml of propylene glycol, 1 to 5ml of water solution of 40 percent PVP[k30], 2 to 6ml of 50 percent water solution of gelatin, 1 to 3.0g of sodium cellulose glycolate, 0.4 to 0.6g of sodium polyacrylate, 1 to 3ml of azone, 0.1 to 0.4g of Ca(OH)2, and 0.1 to 0.4g of Al(OH)3; and the medicine is 0.5 to 3g of andrographolidume, clathrate or solid dispersion containing 0.5 to 3g of andrographolidume. The preparation method comprises the steps of preparing the clathrate and solid dispersion of the andrographolidume, preparing the cataplasm substrate and preparing the cataplasm. The andrographolidume cataplasm and the method have the advantages of overcoming the defects of oral administration and injection administration, avoiding toxic and side effects, ensuring safer administration, improving the bioavailability and making patients administrate medicines more conveniently; moreover, the cataplasm is particularly suitable for the administration of the aged and children.
US6890931 Methods of treating disorders with group I mGluR antagonists Compositions and uses of mGluR5 antagonists for the treatment and prevention of neurological disorders, such as Fragile X, autism, mental retardation, schizophrenia and Down's Syndrome, are disclosed.
WO2006066414A1 Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase Bi-or tricyclic compounds of formula (I) wherein R1, R4 and R5 are as herein defined, A represents a single or double bond and two R2, R2’, R3 and R3’ can be joined to form a condensed or spiro ring. These compounds and their pharmaceutical acceptable salt are used in combinations or pharmaceutical compositions and are useful in methods for preventing or treatin human immunodeficiency virus (HIV) infection or in methods for preventing, delaying or treating acquired immunodeficiency syndrome (AIDS).
US20070160694 Preventives or remedies for tumor or human papillomaviral disease A composition for foods or medicaments, containing a fermentation product or an enzyme-treated product that is either obtained by fermenting or treating with an enzyme at least one type of component selected from the husks, pellicles and astringent skin of Coix seeds.
WO2013006864A2 Treating cancer with hsp90 inhibitory compounds Methods of treating cancer with a compound of formulae (I) or (la) are disclosed. Also provided are methods of treating a cancer with a mutation in ALK or a c-MET mutation with a compound of formulae (I) or (la). Further provided are methods of treating non-small cell lung cancer with a mutation in ALK with a compound of formulae (I) or (la); a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein.
CN101507731A Chitosan uterus-neck antibiotic film and preparation method thereof The invention discloses a chitosan cervical antibacterial film and a preparation method thereof. The preparation method comprises the steps of adopting a formula of gelatin, water soluble chitosan, shell iodine, Tween 80 and glycerol compositions and controlling the pH value, the temperature and the stirring time under the stirring of a vacuum stirrer to prepare a blending polymeric material. The chitosan cervical antibacterial film can maintain the biocompatibility and degradability of original materials, can also ensure that the polymeric material has good bactericidal performance, is used for preventing and treating common gynaecological diseases (cervicitis, after the physiotherapy and surgical treatment of uterine necks), and is a therapeutic biopolymeric material with excellent dual functions of sterilization and repair.
EP1689742B1 Quinolonecarboxylic acid compounds having 5-ht4 receptor agonistic activity This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α1;A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; Rl represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
US20120009278 Composition To Retard the Onset of Symptoms of Alzheimer's Disease Compositions and methods are described for delaying the onset of the symptoms of Alzheimer's disease in humans. The compositions can include curcumin, piperine, oleic acid, oleanolic acid, ursolic acid, galantamine, and huperzine A, among other compounds. Curcumin is an antioxidant, while galantamine and huperzine A inhibit the activity of acetylcholinesterase in the brain. Piperine and oleic acid increase the bioavailability and gastrointestinal absorption of curcumin, galantamine, huperzine A, and other nutrients. The composition can also include at least one of phytic acid, piracetam, aniracetam, or indium.
EP0900235B1 Fragments of cr1 and their use A polypeptide comprising a portion of the sequence of the general formula (I): CNPGSGGRKVFELVGEPSIYCTSNDDQVGIWSG, of 6 to 23 amino acids in length and comprising sequence a) and/or b): a) GGRKVF, b) FELVGEPSIY multimeric and chimaeric derivatives, pharmaceutical compositions containing them and their use in therapy.
CA2759679A1 Novel compound amycolamicin, method for production thereof, and use thereof To provide a new compound having an excellent antibacterial activity against a wide variety of pathogenic bacteria such as drug-resistant bacteria and bacteria causing pneumonia in domestic livestock, tautomers thereof, or salts of the compound or the tautomers; a method for producing them; and the like. A compound having a structure represented by the following Structural Formula (1), tautomers thereof, or salts of the compound or the tautomers; and a method including culturing a microorganism belonging to the genus Amcoylatopsis and capable of producing the compound, the tautomers or the salts, and isolating the compound, the tautomers or the salts from a culture obtained from the culturing; and the like. (see formula 1)
US20100184821 Compositions and Methods for Modulating Angiogenesis The invention generally features compositions and methods that are useful for modulating angiogenesis.
US7388070 inhibitors of DNA polymerase and DNA repair enzymes for treating viral infections, bacterial infections, fungal infections, protozoan infections, and neoplastic diseases; herpes viruses, herpes simplex virus (HSV), and human cytomegalovirus (CMV); peptidomimetics that mimic helical portions of proteins A method for the structure-based identification and selection of inhibitors of processivity factor binding to protein is disclosed herein. Characterization of the protein/processivity factor interface is given. Methods for the structure-based inhibition of processivity factor binding to protein are also given. One embodiment includes a class of peptidomimetics that mimic helical portions of proteins. In addition, methods of treatment of various diseases are given, using the inhibitors of the invention.
US8088921 Method for producing 3-amidinophenylalanine derivatives The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
US6841548 Pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives The invention concerns pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives as active ingredients which carry a group of the general formula R—SO2—O— at their C3 position wherein R is a R1R2N group wherein R1 and R2 are independent of each other and represent a hydrogen atom, a C1-C5 alkyl radical or, together with the N atom, a polymethylene imino radical containing 4 to 6 C atoms, or a morpholino radical. The preparations according to the invention can be used for hormonal contraception and for hormon replacement therapy (HRT). They exhibit a low hepatic estrogenity.
US7820375 Use of a protein of the CRMP family for treating diseases related to the immune system The invention concerns the use of at least a protein of the CRMP family, a polypeptide fragment or an active biological derivative thereof, a nucleotide sequence or sequence fragment coding for said protein, an antisense sequence capable of being specifically hybridized with a sequence with nucleotide-type encoding of said protein or an antibody directed against said protein for producing a medicine for treating diseases related to a dysfunction of the immune system. The invention also concerns a method for diagnosing an autoimmune pathology which consists in measuring the expression of a CRMP protein in the lymphocytes.
WO2014029197A1 3h-1,2-dithiocyclopentene-3-thioketone compounds and application thereof The present invention relates to the field of medicaments, and in particular relates to 3H-1,2-dithiocyclopentene-3-thioketone compounds and application thereof. 3H-1,2-dithiocyclopentene-3-thioketone compounds disclosed by the invention have new structures shown in formula I or formula II. Proved by experiments, 3H-1,2-dithiocyclopentene-3-thioketone compounds can directly protect neurons on a cell model, and can significantly restrain excessive inflammatory responses of inflammatory cells in the cerebrum; and by using 3H-1,2-dithiocyclopentene-3-thioketone, focal cerebral ischemia cerebral infarction volume of a mouse can be obviously reduced in an animal model. Therefore, the invention provides the application of 3H-1,2-dithiocyclopentene-3-thioketone compounds and pharmaceutically acceptable salts thereof in the preparation of medicaments for preventing or treating cerebral apoplexy diseases.
CN103751166A Application of benzyl-4-(benzyloxy)-dimethoxy benzoate in preparation of drugs for preventing and treating rheumatoid arthritis The invention relates to the field of drugs, and particularly relates to a compound capable of inhibiting proteasomes and preventing and treating rheumatoid arthritis. The compound has the molecular structure of benzyl-4-(benzyloxy)-dimethoxy benzoate. The compound has the beneficial effects that the compound can be used for treating rheumatoid arthritis, and has potential new drug development value.
CN103435594A 2-amino-quinazolines PLK1 (Polo-like kinase1) inhibitor and application thereof The invention relates to the field of medicinal chemistry, and particularly relates to 2-amino-quinazolines compounds, preparation methods of the 2-amino-quinazolines compounds, medicinal compositions containing the compounds, and medical applications of the 2-amino-quinazolines compounds and the medicinal compositions, especially applications of the 2-amino-quinazolines compounds and the medicinal compositions serving as Polo-like kinase1 inhibitors.
WO2013186666A1 Tricyclic compounds as kat ii inhibitors Compounds of Formula (I), wherein R1, R 2, X1, Y1, Z1, and Z2 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
CN1957936A Silybin tiny pellets and preparation method A micropill of silibinin is prepared through dissolving silibinin and high-molecular material in a solvent, suspending an insoluble material in obtained solution, adding a poor solvent to form a sub-stable emulsion in which said solution is internal phase and said poor solvent is external phase, continuous diffusion of better solvent in emulsion drops while educing out medicine and high-molecular material and depositing them on the internal and external surfaces of disperser, adding the bridging liquid, and stirring.
WO2007130353A3 Phase 2 inducers, ppar-alpha agonists and related signalling pathways protect cartilage against inflammation, apoptosis and stress Disclosed herein are novel compounds, their use in the treatment and prevention of joint and/or cartilage inflammation that provide an alternative to the NSAIDS and selective COX-2 inhibitors by activating endogenous detoxifying cellular defense mechanisms that act to neutralize toxic cellular intermediate. These compounds are PPAR-alpha agonists and/or phase 2 gene activators.
WO2006095074A1 Anti-smoking composition The invention concerns an anti-smoking composition for reducing or suppressing addiction to cigarette smoking, and designed to be incorporated in nutritional supports containing: dextrose or at least one constituent comprising dextrose formulated into a tablet resisting to a force of intensity ranging between 170 and 250 N, of diameter between 20 and 25 mm, of thickness between 5 and 10 mm and weighing between 2.7 and 3.0 g; and at least one constituent including in particular a combination of linoleic and linolenic acid in a weight ratio of 3/1 to 6/1.
CN101856334A Asarin composite freeze-dried powder for injection The invention relates to an asarin injection preparation and in particular relates to an asarin composite aseptic freeze-dried powder preparation for injection. The asarin composite freeze-dried powder for injection comprises 4 to 8 grams of asarin, 40 to 80ml of ethanol of which the volume ratio is between 95 and 100 percent and 24 to 80 grams of mannitol. The raw materials is added with water for injection to a volume of 1,000 to 2,000ml and the obtained product is freeze-dried to prepare 500 to 1,000 bottles of the freeze-dried powder, wherein the asarin is ultrafine particles prepared by an anti-solvent crystallization method. The asarin composite preparation for injection also comprises 0.01 to 10 grams of polysorbate-80, preferably 1 to 8 grams of polysorbate-80. Due to adoption of the ultrafine particles of the asarin, which is prepared by the anti-solvent crystallization method, the asarin composite aseptic freeze-dried powder preparation for injection greatly improves solubility property of the asarin so as to obtain the freeze-dried powder preparation with excellent stability and redissolution property by adding a small quantity of cosolvent or without adding the cosolvent when preparing the asarin preparation.
WO2008096122A2 Progesterone for the prevention of preterm birth A method for treating or preventing spontaneous preterm birth in pregnant women and improving neonatal morbidity and mortality. The method includes administering to a pregnant woman in need thereof an effective amount of a progesterone sufficient to prolong gestation by minimizing the shortening or effacing of her cervix. Treatment and prophylaxis with progesterone in pregnant women having symptoms of short cervix has been clinically shown to increase neonatal health.
CN1837226B Separation of medical derivatives from phoenix-tail fern and use thereof The invention relates to relates to Yangqinzisu-4'-alphs-L- rhamnoside, a novel glucoside of Yangqinzisu extracted from phoenix-tail fern. Tests show that, the Yangqinzisu-4'-alpha-L-rhamnose-7-beta-D-heteroside and docosanoic acid has very strong inhibitory action to the proliferation of cultivated prostate gland cells, thus can be applied into the development of medicaments for treating prostatehyperplasia and prostatitis.
CN101139368A Histone deacetylase inhibitor organic tin polyacid compound and preparation method thereof The present invention belongs to multi-acid compounds and related synthetic method, which especially relates to a group of histone deacetylase inhibitor organic tin multi-acid compound and the related acid synthesis method. The preparation method is to respectively dissolve a certain amount of three-absenece Keggin heteropoly tungstenK10[A-GeW9O34]question mark 25H2O, K10[A-SiW9O34]question mark 25H2O, K9[A-AsW9O34]question mark 25H2O, K9[A-SbW9O34]question mark 25H2O or K9[A-PW9O34]question mark 25H2O into the HAc-NaAc buffer solution of 1 mol per L, and then modest single-butyl tin is added for reaction under heating. A plurality of drops of 1 mol per L KCl solution are added, and then the solution is cooled and filtered. The main mechanism of the product is to cure the cancer through the inhibiting of histone deacetylase and the avoidance of gene expression suppression due to the foul-up of histone deacetylase collection function.
CN1839800A Vinorelbine Bitartrate lipsome freeze-drying powder injection and its preparation method The invention relates to an antineoplastic vinorelbine bitartrate liposome, its freeze-dried powder injection and preparing process, wherein the preparation comprises liposome of vinorelbine bitartrate and pharmaceutically acceptable carrying agent, the liposome of vinorelbine bitartrate contains the following constituents: vinorelbine bitartrate, phosphatide, cholesterin and vitamin E, their weight ratio being 1 : 1-100 : 1-15 : 0.01-0.05.
WO2009084497A1 Methyl-substituted piperidine derivative Disclosed is 2-({6-[(3R)-3-amino-3-methylpiperidin-1-yl]- 1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl}methyl)-4-fluorobenzonitrile having high DPP-IV inhibitory activity and improved safety and toxicity, or a pharmaceutically acceptable salt thereof.
WO2011082519A1 Geldanamycin derivatives, preparation methods and uses thereof Geldanamycin derivatives, preparation methods and uses thereof in the manufacture of medicaments of cell killing agents, cell proliferation inhibitors and antitumor agents are disclosed.
CN103191285A Externally used drug for treating bone traumas and preparation method of externally used drug plaster for treating bone traumas The invention provides an externally used drug for treating bone traumas and a preparation method of the externally used drug plaster for treating bone traumas, relating to externally used drugs and solving the problems that the bone trauma treatment effect is poor and technology is insufficient. The externally used drug for treating bone traumas is mainly prepared from 200g of withy, 200g of giant knotweed rhizome, 100g of sappan wood, 100g of rhizoma paridis Yunnanensis, 30g of erodium stephanianum willd, 30g of Chinese angelica, 20g of cochinchina momordica seed, 20g of Chinese honeylocust spine, 20g of pangolin scales, 10g of hair, 20g of dragon blood, 20g of frankincense, 20g of myrrh, 30g of cutch, 20g of Chinese asafoetida, 10g of knoxia corymbosa willd, 10g of borneol, 20g of rosin, 20g of zinc oxide, 250g of sesame oil and 1000g of rubbers. The externally used drug plaster prepared by the invention is mainly used for treating traumatic injuries, fractures, joint effusion, sore toxin, arthritis, lumbar disc herniation, cervical spondylosis and gout.
WO2005102388A1 Novel blt2-mediated disease, and blt2 binding agent and compound [PROBLEMS] It is demanded to provide a compound capable of selective binding to BLT2 and to provide a preventive and/or therapeutic agent for cutaneous disease and other BLT2-mediated diseases. [MEANS FOR SOLVING PROBLEMS] There is provided a compound having the activity of binding to BLT2, its salt or solvate, or a prodrug thereof. The compound having the activity of binding to BLT2, especially compound of the general formula: (I) (wherein the characters have the same meaning as mentioned in the description), its salt or solvate, or a prodrug thereof, because of having the activity of binding to BLT2, is useful as a preventive and/or therapeutic agent for BLT2-mediated diseases, such as cutaneous disease, bowel disease, HIV infection, transplant rejection, transplanted organ ablation, graft-versus-host disease, autoimmune disease, allergic disease, inflammation, infectious disease, tumor, lymphoma, malignant tumor, leukemia, arteriosclerosis, hepatitis, liver cirrhosis and cancer.
WO2013170757A1 4-aminoquinazoline hydroxamic acid compound and application as antineoplastic medicament Provided is a 4-aminoquinazoline hydroxamic acid compound as represented by formula (V) or a pharmaceutically acceptable salt thereof. The compound provides great histone deacetylase inhibitory activity, great inhibitory activities against various tumor cells of the human body, weak inhibition against normal cells, and reduced toxicity, and is applicable for development as an antineoplastic medicament. In addition, the compound also provides great efficacy in the treatment of diseases induced by abnormal gene expression.
US20130045991 Neuroprotective modulation of nmda receptor subtype activities In various aspects, the invention provides methods and compositions for modulating NMDA receptor subtype activity, to enhance NR2A-containing NMDA receptor activity relative to NR2B-containing NMDA receptor activity, so as to effect a neuroprotective reduction in excitotoxic NMDA receptor activity
US7186730 Bicyclic nitrogen-containing heterocyclic derivatives for use as antibacterials Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
CN102958908A New polymorphic form of calcimimetic compound The present invention relates to the crystalline, polymorphic Form X of the calcimimetic compound {4-[(1R, 3S)-3-((R)-1 -Naphthalen-1 -yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form X by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1 -Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in a C1-C6 alkyl alcohol, or alternatively by precipitation from a neutralized saponification reaction mixture following the alkaline hydrolysis of a C1-C6 alkyl ester of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.
CN100998592A Microemulsion containing matrine A microemulsion of matrine with high biologic utilization rate and stability is proportionally prepared from matrine, emulsifier, emulsifying aid, oil phase and water phase. Its preparing process is also disclosed.
EP1692114A1 Novel benzimidazole and imidazopyridine derivatives and use thereof as a medicament The invention relates to novel benzimidazole and imidazopyridine derivatives having general formula (I), which have a good affinity with certain sub-types of melanocortin receptors, particularly MC4 receptors. Said derivatives are particularly suitable for the treatment of pathological states and diseases involving one or more melanocortin receptors. The invention also relates to pharmaceutical compositions containing said products.
EP1954692A1 Heterocycle-substituted 3-alkyl azetidine derivatives Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CBl) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CBl receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro- inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
US20080221178 Benzimidazole Derivatives,Compositions Containing Them, Preparation Thereof and Uses Thereof Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3 and Ar are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
US20090264380 6,11-bridged biaryl macrolides The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
US20060216317 Delivery of polynucleotide agents to the central nervous system The present invention provides a method for delivering polynucleotide agents, particularly oligonucleotides, to the CNS of a mammal by way of a neural pathway originating in the nasal cavity or through a neural pathway originating in an extranasal tissue that is innervated by the trigeminal nerve.
EP2056880A1 Nucleic acid modulation of toll-like receptor-mediated immune stimulation The present invention provides methods of modulating the activation of certain Toll-like receptors (TLRs) such as TLR7/8 using chemically modified nucleic acid molecules. The present invention also provides methods of using such modified nucleic acid molecules to treat diseases or disorders associated with TLR7/8 activation such as systemic lupus erythematosus. The present invention further provides compositions comprising a combination of modified nucleic acid molecules and nucleic acid molecules that silence expression of one or more target sequences. Methods of using such compositions to reduce or abolish target gene expression without inducing cytokine production are also provided.
US20100104636 Pharmaceutical Compound and Composition A pharmaceutical composition comprising rosiglitazone or a pharmaceutically acceptable salt thereof wherein said rosiglitazone has a median particle size diameter of about 5 microns to about 20 microns.
CN102631470A Ejiao Guiqi granules and manufacturing method thereof The invention relates to Ejiao Guiqi Granules and a manufacturing method of thereof. The Ejiao Guiqi granules belong to health foods and have the function of improving alimentary anemia. The Ejiao Guiqi granules comprise the following active ingredients by weight: 30-80 parts of donkey-hide gelatin; 20-50 parts of codonopsis pilosula; 10-40 parts of padix rehmanniae preparata; 20-40 parts wolfberry fruit; 20-40 parts of rhizoma atractylodis macrocephalae; 1-4 parts of vitamin C; 0.5-2 parts of ferrous lactate; and 750-1000 parts of white sugar. The Ejiao Guiqi granules are manufactured through the processes such as melting the donkey-hide gelatin by heat, boiling codonopsis pilosula, padix rehmanniae preparata, wolfberry fruit and hizome atractylodis macrocephalae with water for extraction, performing vacuum concentration, ethanol precipitation and ethanol recovery, mixing, granulating, drying, grading, packing and the like. The Ejiao Guiqi granules have the characteristics of scientific formulation, reasonable process and the like. Through human body tests, the Ejiao Guiqi granules are proven to have functions of improving alimentary anemia and promoting health, have no adverse effect on health, and are safe and reliable to eat.
CA2722112A1 Treating eosinophilic esophagitis This document provides methods and compositions suitable for treating eosinophilic esophogitis. For example, this document provides methods that involve administering a steroid and mucoadherent to a mammal (e.g., a human). Kits comprising compositions containing a steroid in combination with a mucoadherent also are provided.
WO2009051659A3 Therapeutic sirna molecules for reducing vegfr1 expression in vitro and in vivo The invention relates to nucleic acid molecule compositions for use in modulating the expression and activity of VEGF pathway genes and decreasing unwanted neovascularization, including tumor angiogenesis, by RNA interference and methods and compositions comprising the nucleic acid molecules.
US20110028412 Herbal enhanced analgesic formulations The analgesic properties of L-tryptophan and 5-HTP can be safely enhanced with the coadministration of salacin. Salacin can be effectively provided in the form of white willow bark along with other ingredients to further enhance the formulation's analgesic effect. As salacin can cause the loss of vitamin C in humans, the formulation advantageously includes a supplemental amount of vitamin C.
US7060731 Such as meglumine, 3-methylamino-1,2 propandiol or 2-(methylamino)-ethanol as complement inhibitors, to combact activation of the kinin/kallikrein system or as an anticoagulant This application relates to the use of certain amines of formula (I) for combatting and preventing systemic and local complement activation, and in particular to the use of meglumine and derivatives and optionally salts thereof in combatting and preventing said activation. The amines are also of use in combatting activation of the kinin/kallikrein system or blood coagulation system.
US6875792 Inhibition of glutamine synthetase; antiswelling and antiepileptic agents Methods for the treatment of both diseases susceptible to the inhibition of mammalian glutamine synthetase and progressive hyperammonemic encephalopathy comprising administering L-methionine S-sulfoxime at a dose not to exceed 10 mg/kg body weight are disclosed. Preferably, the dose should not exceed 8 mg/kg; more preferably, the dose should not exceed 5 mg/kg; most preferably, the dose should not exceed 2.5 mg/kg.
EP1220675B1 Hormone-sensitive lipase activity mediated male infertility In various aspects, the invention provides pharmacologic and genomic methods of inhibiting fertility in a male animal, such as human male contraception, involving the manipulation of the activity of hormone-sensitive lipase, including inhibiting the activity of a hormone-sensitive lipase in the animal. In another aspect, the invention discloses the use of hormone-sensitive lipase as a target in screening assays that may be used to identify compounds that modulate male fertility. In another aspect, the present invention identifies a condition of male infertility caused by hormone-sensitive lipase deficiency.
CA2369448C Medicament for inhibiting nf-kb Compounds of formula (I) (see formula I) wherein R1 through R8 are selected independently from hydrogen atoms and pharmaceutically acceptable substituents, as well as pharmaceutically acceptable salts of compounds of formula (I) and mixtures of substances containing at least one compound of formula (I) or a pharmaceutically acceptable salt thereof are used for preparation of medicaments for inhibiting transcription factor NF-.kappa.B and/or for inhibiting COX with a preferential inhibitory effect for COX-2.
US6992072 comprises pyrimidine-based nucleosides; highly active anti-retroviral therapy; treating lipoatrophy, dyslipidemia, and insulin resistance resulting from administration of nucleoside reverse transcriptase inhibitors The invention relates to the use of active ingredients, which increase the concentration of pyrimidine-based elements for nucleic acid biosynthesis in the body, in particular to the use of pyrimidine nucleosides and/or prodrugs produced therefrom, for reducing the side-effects of inhibitors of nucleic acid biosynthesis or their precursors, in particular by activating the biosynthesis of mitochondrial DNA (mtDNA). The invention also relates to the use of said active ingredients, in particular pyrimidine nucleosides and/or prodrugs for producing pharmaceutical preparations for reducing the aforementioned side-effects and to combinations or products for administering active ingredients of this type, in particular pyrimidine nucleosides and/or prodrugs produced therefrom, comprising inhibitors of nucleic acid biosynthesis or their precursors. The invention further relates to methods for treating the side-effects of inhibitors of nucleic acid biosynthesis or their precursors using the aforementioned active ingredients, in particular pyrimidine nucleosides and/or prodrugs produced therefrom, or the aforementioned combinations or products and to corresponding pharmaceutical preparations. Side-effects of HAART (Highly Active Anti-Retroviral Therapy) and side-effects of other anti-viral nucleoside analogous agents, which inhibit the mitochondrial γ-polymerases, can in particular be prophylactically and/or therapeutically treated in this manner.
CN102274228B Compound trimethoprim and sodium succinate florfenicol nanoemulsion preparation and preparation thereof The invention belongs to the technical field of antibacterial veterinary drugs, and in particular relates to a compound trimethoprim and sodium succinate florfenicol nanoemulsion preparation. The nanoemulsion preparation is in an oil-in-water type, has the grain size of between 1nm and 100nm and is prepared from trimethoprim, sodium succinate florfenicol, a surfactant, a cosurfactant, oil and distilled water. The compound trimethoprim and sodium succinate florfenicol nanoemulsion preparation has transparent appearance and can be used for treating various livestock and poultry infections caused by sensitive bacteria.
CN102784352A Agent for treating psoriasis vulgaris The invention relates to an agent for treating psoriasis vulgaris, and specifically to an external application agent for treating psoriasis vulgaris. A purpose of the present invention is mainly to solve problems of low cure rate and easy recurrence of external application agents for treating psoriasis vulgaris in the prior art. A formula of the agent of the present invention comprises: 5 g of musk, 25 g of borneol, 25 g of radix notoginseng, 50 g of sulfur, 50 g of realgar, 25 g of rheum, 25 g of angelica, 20 g of salvia miltiorrhiza, 18 g of amur corktree bark, 15 g of coptis chinensis, 25 g of frankincense, 25 g of angelica archang lica, 20 g of licorice root, 16 g of weeping forsythia fruit, 17 g of glabrous greenbrier rhizome, 15 g of honeysuckle, 25 g of balloonflower root, 21 g of seasoned orange peel, 13 g of blue turmeric rhizome, 21 g of arborvitae, 9 g of mythic fungus, 17 g of tribulus terrestris, 16 g of tuber fleeceflower root, 22 g of dandelion, and 18 g of folium isatidis. According to the preparation method, the materials in the formula are mixed and added with water, wherein the amount of the water is 10 times the total weight of the materials; boiling is performed for one hour; filtration is performed to obtain the primary resulting drug liquid; water is added to the boiled materials, wherein the amount of the water is 10 times the total weight of the materials; then boiling is performed for one hour; filtration is performed to obtain the secondary resulting drug liquid; and the primary resulting drug liquid and the secondary resulting drug liquid are mixed. The agent of the present invention has advantages of high cure rate and less recurrence.
US20110112176 Compositions and methods for inhibiting expression of kif10 genes The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a KIF10 gene. The invention also relates to a pharmaceutical composition comprising the dsRNA or nucleic acid molecules or vectors encoding the same together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of a KIF10 gene using said pharmaceutical composition; and methods for inhibiting the expression of KIF10 in a cell.
US7829596 administering to the patient an effective amount of a xanthine oxidase inhibitor ( allopurinol, 7,8-dihydroneopterin, 5,6,7,8-tetrahydrobiopterin, leukopterin, xanthopterin, neopterin etc.) to reduce sympathetic nervous system activity and/or improving cardiovascular reflex status for treating cachexia A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a β receptor blocker; an imidazoline receptor antagonist; a centrally acting α receptor antagonist; a peripherally acting α receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduces SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidize inhibitor. The methods are particularly useful in treating cardiac cachexia.
US20090163509 Method for healing a wound using an alpha-adrenergic antagonist A method for healing a wound comprising the step of topically administering a wound healing composition to a wounded area, wherein the wound healing composition comprises a first medicament characterized as an alpha-adrenergic antagonist and pharmaceutically acceptable salts thereof.
US20080200553 N-[2-Chloro-4-pentafluorosulfanylbenzoyl]guanidine; ischemia, reperfusion, arrythmia angina pectoris; inhibit the cellular sodium-proton antiporter (Na+/H+ exchanger, NHE); stability, longer half-life in vivo, high bioavailability Pentafluorosulfanylbenzoylguanidines of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.
CN102206139A Kaurane compound, and preparation method and purpose thereof The invention relates to a kaurane compound, and provides a preparation method and a purpose of the compound. The disclosed kaurane compound is a white powdery matter with a chemical name of ent-kauran-3beta,16beta-17-,19-tetrol, and a molecular formula of C20H34O4. Smallanthus sonchifolius leaves are processed through a rough extraction. The crude extract is processed through a macroporous resin column chromatography, a silica gel column chromatography and a reversed-phase C18 column chromatography, such that a kaurane compound crude product is obtained. A high-efficiency liquid-phase preparation is then carried out, such that a kaurane compound is obtained. Through extraction and separation, the new kaurane compound is obtained from smallanthus sonchifolius leaves. The compound can effectively inhibit the activity of alpha-glucosidase. 1.6mg/ml of the compound contributes in achieving an alpha-glucosidase inhibition rate of about 70%. Therefore, with a good blood glucose reducing effect and a good anti-diabetes effect, the compound can be widely applied in the preparation of medicines against uretic diseases, and has potentials to be exploited in the production of anti-diabetes medicines.
US20130035309 Ophthalmic sealant composition and method for use A polymeric hydrogel sealant specifically formulated to seal ophthalmic wounds is provided. The sealant is formed by mixing two aqueous solutions. The first aqueous solution comprises an oxidized dextran having a specific average molecular weight range and oxidation level and the second aqueous solution comprises a 4-arm polyethylene glycol having two primary amine groups at the end of substantially every arm. A kit and method for sealing an ophthalmic wound using the hydrogel sealant is also provided.
WO2013156871A3 Thromboxane receptor antagonists The invention generally relates to compounds that function as TP antagonists for treating thrombosis and other cardiovascular, renal, or pulmonary diseases. In some embodiments, the invention provides a compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group. In some embodiments, the invention provides a method of treating thrombosis by administering an antithrombotic compound that preferentially binds to a thromboxane receptor, has preferential binding for either TPalpha (TPα) or TPbeta (ΤΡβ) receptor subtype.
WO2013000108A1 Azole heterocylic compounds, preparation methods, pharmaceutical compositions and uses thereof Provided are azole heterocylic compounds of formula (I) or formula (II), their preparation methods, their pharmaceutical compositions and their use in the preparation of medicaments for treating diseases associated with the enzyme Lp-PLA2, wherein the definitions for each substituent are same as described in the description.
WO2009111064A2 Minocycline compounds and methods of use thereof Methods and compositions for using a tetracycline compound to treat bacterial infections are described. In one embodiment, for example, the invention provides a method of treating a subject for an infection, comprising administering to said subject an effective amount of 9- [(2,2-dimethyl-propyl amino)-methyl]-minocycline or a salt thereof, such that said subject is treated, wherein said infection is selected from the group consisting of MSSA, MRSA, B- streptococci, Viridans Streptococci, Enterococcus, or combinations thereof.
US20120225049 Fast acting snare-cleaving enzymes The present invention relates to metalloprotease enzymes isolated from scorpion venom, their nucleic acid and amino acid sequences, and methods of use thereof in the treatment of various diseases, disorders and cosmetic conditions.
CA2787078A1 Methods for internally controlling or treating equine bot larvae Provided are novel methods and formulations for orally controlling bot larvae in the gastrointestinal tract of equine animal.
WO2012154698A2 Method to improve antiviral activity of nucleotide analogue drugs A method of modifying a nucleotide or a nucleotide analogue to increase its overall effectiveness in treating an antiviral disease is provided. In some cases, a compound comprising a base, sugar, phosphonate moiety, and amino acid residue is provided, where the base-sugar may be a nucleoside, and the amino acid residue may be a tyrosine residue. In certain cases, the tyrosine residue contains a long chain alkyl group on the carboxamide group of the residue. Methods of inhibiting viral replication and methods of treating a viral infection are also provided.
EP1557167A1 Viral inhibition by long-chain alcohols alkanes fatty acids and amides There are disclosed compositions for theraputic use comprising a mixture of from 1:1 (w:w) to 10:1 (w:w) of a nonionic surfactant and an active ingredient in a pharmaceutically acceptable diluent or carrier, wherein the nonionic surfactant is a deoxycholate and wherein the active ingredient is selected from the group consisting of stearyl alcohol, erucyl alcohol, brassidyl alcohol, n-docosanol, arachidyl alcohol, n-docosane, n-docosanoic acid erucamide, stearic acid, or mixtures thereof.
CN101703541B Four-species medicinal powder for treating leukoderma The invention relates to a four-species medicinal powder for treating leukoderma, which is oral administration powder prepared by four species of tribulus terrestris, borneol and the like. The medicinal powder has pungent, bitter and mild taste and has no toxic and side effect. The four-species medicinal powder for treating leukoderma has the functions of promoting blood circulation, clearing up blood stasis, dispelling cold, relieving exterior syndrome, dispelling wind and arresting itching, reducing the humidification, controlling leucorrhea, relieving convulsion, soothing the nerves, delaying gastrointestinal motility, soothing the liver, relieving depression, improving eyesight, reducing weight, activating hypoderm sympathetic system hormone, promoting release of the kidney cortex in order to decompose subcutaneous fat protease and exciting medulla blood vessel motion pivots in order to promote the increase of blood plasma adrenal corticosterone and the rebirth of the red blood cells and hemoglobin, so that the medicinal powder has specific treatment effect on the hypoderm spreading type leucoderma. The medicinal powder needs to be taken three times a day, 6 to 10 grams for each time, and the medicinal powder is taken 30 minutes before meals after mixed with hot water or hot water. The medicinal powder can not be taken with acid and alkali food, gallbladders, preserved food, pungent food, peppery food, and high protein food, can not be mixed with Western hormonemimic medicine, or can not be taken by people with stagnancy of Qi and blood and gravida.
WO2012130306A1 Bicyclic 2,3-dihyrdobenzazine compounds for use in therapy The present invention provides novel 2,3-dihydrobenzazine compounds of formula (I) and to their salts. The compounds inhibit cell proliferation and cell division and they also inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions (I) wherein X is O or S(=O)n; n is 0, 1 or 2; R1 is an optionally substituted C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring having either 1, 2 or 3 nitrogen atoms as heteroatom ring members or 1 oxygen or 1 sulfur atom and 0, 1 or 2 nitrogen atoms as heteroatom ring members, and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring having 1, 2 or 3 heteroatom ring members selected from oxygen, sulfur and nitrogen, where sulfur atoms, if present, may be present as S, S(O) or S(O)2 and where the saturated or unsaturated carbocyclic or heterocyclic second ring may also have 1 or 2 carbonyl groups or thiocarbonyl groups as ring members; R2 is an optionally substituted aromatic radical selected from phenyl, C-bound mono- cyclic 5- or 6-membered heteroaryl or C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring.
US20080254015 For application to wounds; bacteriostats A gel for application to a wound, comprising a mixture of citrus complex carbohydrates, a cellulose derivative, a polyol component and water, wherein said citrus complex carbohydrates are cross-linked to said cellulose derivative by an ionic cross-linking agent.
US20120053136 Diagnosis and treatment of drug-resistant ewing`s sarcoma Disclosed herein are diagnostic and prognostic methods for determining drug sensitivity and resistance in Ewing's sarcoma patients. Treatments for drug-resistant Ewing's sarcoma are also disclosed. The assays involve the detection of GSTM4 gene expression alone or in combination with other clinical factors. The tests are suitable for diagnosing and monitoring treatment of patients having or suspected of having Ewing's sarcoma. The disclosure also relates to inhibitors of GSTM4 for the treatment of Ewing's sarcoma, including drug-resistant forms thereof.
US20060078626 Opthalmic and contact lens solutions with a peroxide source and a cationic polymeric preservative An ophthalmic solution including 0.01 to 0.0001 percent by weight of a peroxide producing agent and 0.1 to 500 parts per million of a cationic, polymeric preservative.
CN101817805A Andrographolide derivative and preparation method and application thereof The invention discloses an andrographolide derivative and a preparation method and application thereof. The derivative has a structure expressed by the formula (1), wherein R1 is C1 to C11 chain hydrocarbon or C1 to C11 chain hydrocarbon with terminals substituted by ternary to heptabasic ring groups; and R2 and R3 are hydrogen, organic acid radical, inorganic acid radical, alkyl or acryl. The andrographolide derivative can be made into tablets, capsules, granules, fine granules, powder, pills, patches, oral liquid or injection.
CN102920833A Externally applied medicine for curing prostatitis The invention discloses externally applied medicine for curing prostatitis. The medicine is composed of a first group of active pharmaceutical ingredients (APIs) and a second group of APIs, wherein the first group of APIs comprises cassia twig, licorice and the like; and the second group of APIs comprises amur cork tree bark and the like. The medicine comprises more than thirty medicinal materials such as red flower and the licorice, producing time is long, and properties of the medicine are fully induced through a fermentation process, so that penetration of the medicine is strengthened; the medicine is soaked by rice wine alcohol which can induce efficacy as a medicinal inducer in itself; and gauze is soaked by liquid medicine, ointment is matched for use, the efficacy is further strengthened, curing time is shortened, and properties of the ointment are fully played. The reactions of users are obvious during usage, effects of the medicine are remarkable, and the medicine can eliminate diseases and radically treat sickness through reasonable use.
US20120010206 Imidazolopyridine compounds useful for the treatment of degenerative and inflammatory diseases Novel imidazolopyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, ECM degradation, joint degradation and/or inflammation, and others.
US20100323965 Thrombopoietin Mimetics The invention relates to compounds and their use in the treatment of thrombocytopenia resulting from diseases or conditions such as immune thrombocytopenic purpura, cancer chemotherapy, surgery, bone marrow or stem cell transplantation, radiation injury or treatment, chronic viral infection, and pancytopenia. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods for treating such diseases or conditions in a mammal, including a human, by administering to such mammal an effective amount of a selected thrombopoietin receptor agonist.
US20070219114 Preventives or Remedies for Hepatopathy The present invention relates to a preventive or a therapeutic agent for hepatopathy, comprising, as an effective ingredient, a polypeptide derivative having an activity of binding to growth hormone secretagogue receptor and thus elevating intracellular calcium ion concentration, and having one amino acid sequence selected from the group consisting of amino acid sequences represented by SEQ ID NOS: 1 to 22, or an amino acid sequence in which one to several amino acids are deleted, substituted or added at the amino acid residues other that the first to forth amino acid residues from the amino-terminus in the said amino acid sequence, or a pharmacologically acceptable salt thereof. The preventive or the therapeutic agent for hepatopathy in accordance with the present invention is useful as a drug suitable for treating or preventing hepatic diseases such as hepatitis, liver cirrhosis and hepatic insufficiency. Further, the preventive or the therapeutic agent for hepatopathy in accordance with the present invention is also useful as an agent of promoting hepatic regeneration and hepatic function recovery after hepatectomy.
CA2474460C Pyridine- and quinoline-derivatives The present invention relates to compounds of formula (I), wherein R1, R2, R3 and R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
WO2013025064A2 Anti-cancer composition comprising wnt decoy receptors The present invention relates to a composition for preventing or treating cancer, comprising Wnt decoy receptors as active ingredients. The composition or expression products thereof according to the present invention are bound to Wnt ligands to block ligand-receptor interactions, thereby inhibiting carcinogenesis and the growth, proliferation, and metastasis of cancer and inducing apoptosis in cancer cells, and thus may be valuably used as an efficient anti-cancer composition.
CN101254287A Medicament containing aminoglucose and uses thereof The invention discloses a drug containing glucosamine and an application thereof, and the drug is glucosamine or includes glucosamine and chitosan or the extracts of turtle shell, common yam rhizome and malt. Wherein, the weight percentage content of the glucosamine is 50 percent to 100 percent, the weight percentage content of the extracts of the turtle shell, the common yam rhizome and the malt is 0 to 50 percent, or the weight percentage content of the glucosamine in the drug is 50 percent to 100 percent, and the weight percentage content of the chitosan is 0 to 50 percent. The invention relates to the application of the glucosamine drug composition in the preparation of the drugs for promoting the growth and the development, the growth and the development can be promoted by taking a small amount of the drug composition every day, which further has no toxicity or side effects.
CN101768170A Cefathiamidine hydrate, preparation method thereof and application thereof The invention relates to a cefathiamidine hydrate, a preparation method thereof and application thereof. The crystalline hydrate has high storage stability, and is applicable in preparing medicaments for treating or preventing gram positive or negative bacteria sensitive bacteria, infections of human or animal respiratory system, liver and biliary system, five sense organs and urogenital system, bone and joint infection and soft skin tissue infection caused by the gram positive or negative bacteria sensitive bacteria, and diseases such as endocarditis, ichorrhemia, meningitis and the like.
WO2013158698A3 Method treating scleroderma The present invention provides a method for treating scleroderma by administering a therapeutically effective amount of a toll like receptor 4 inhibitor to a subject in need of such a treatment.
US20100137289 Methods and Compositions for Ameliorating Thiazide Induced Hyperlipidemia Male Disclosed herein are compositions for ameliorating the lipid producing effects of thiazide therapy. Particularly exemplified herein are compositions containing a thiazide and allopurinol, or some other xanthine oxidase inhibitor.
CN1813759A Promethazine hydrochloride dropping pill and its preparing method The present invention discloses a kind of promethazine hydrochloride dripping pills for curing anaphylactic diseases of skin and mucosa, etc. and kinetosis and its preparation method. It is made up by using promethazine hydrochloride and dripping pill matrix through a certain preparation process. Its bioavailability is high and its medicine stability is good.
CN101129347A Florfenicol oil emulsion injection and method for formulating the same The invention discloses a fluorobenzene nikao oil-emulsion injection and dispensing method, which comprises the following parts: 9. 8-10. 2% fluorobenzene nikao, 1-2% tween-80, 3-4% sibenzene-80, 35-40% injecting soy oil and 45-50% injecting water. The making method comprises the following steps: dissolving the fluorobenzene nikao and sibenzene-80 proportionally and sterilizing under high temperature and high pressure as oil phase; adding tween-80 into the injecting water to sterilize under high temperature and pressure as water phase; fetching equal quantity of the oil phase and water phase to emulsify sufficiently for 10-15 min; adding the injecting water sterilized under high temperature and pressure to obtain the product with final density at 9. 8-10. 2%; sucking through silk sieve; packing in the sterilized ampoule.
CN103623066A Corydalis impatiens total alkaloid extractive for preparing anti-cancer drugs and application thereof The invention discloses corydalis impatiens total alkaloid extractive for preparing anti-cancer drugs. The content of total alkaloids in the discloses corydalis impatiens total alkaloid extractive is not less than 50wt percent; the disclosed corydalis impatiens total alkaloid extractive comprises 10 to 12wt percent of protopine, 8 to 10wt percent of alpha-bicuculline and 10 to 15wt percent of ochotensimine; the extracting steps of the extractive comprise grinding corydalis impatiens drugs, performing reflux extraction to the corydalis impatiens drugs through saturated alkaline ethyl alcohol or saturated alkaline methyl alcohol, and concentrating and trying the corydalis impatiens drugs, so as to obtain corydalis impatiens extractive, then dissolving and filtering the extractive through acid solution, adding alkali solution into filter liquor, and adjusting the pH value of the solution to be 9 to 10, so as to obtain acid and alkali treated fluid, adding organic solvent into the acid and alkali treated fluid, so as to perform extraction, obtaining corydalis impatiens total alkaloid crude extract, and then purifying the corydalis impatiens total alkaloid crude extract, so as to obtain the corydalis impatiens total alkaloid extractive. The corydalis impatiens total alkaloid extractive obtained through the method has effects of breast cancer resistance, ovarian cancer resistance, stomach cancer resistance and lung cancer resistance.
CN102671197A Medical composite containing deoxidation phenylephrine The invention relates to a medical composite containing deoxidation phenylephrine. The deoxidation phenylephrine and another antihistamine medicine are used as active components so as to be mixed with pharmaceutically acceptable auxiliary materials to form the medical composite. The composite can be prepared into oral preparations including a tablet, a capsule, an effervescent tablet, a chewable tablet, a sustained release tablet, a sustained release capsule and the like, and can be used for releasing relative symptoms of seasonal allergic rhinitis and common cold.
US7368448 2-(arylalkoxy)-1-phenylethylamine derivatives as NK1 antagonist and serotonin reuptake inhibitors Compounds of the following formula (I) wherein R1 R2, n, Ar1 and A2 are as defined in the specification, in vivo-hydrolysable precursors thereof, pharmaceutically acceptable salts thereof, the use in therapy and pharmaceutical compositions and methods of treatment using the same. The example compounds are 1-(2-(naphthylmethoxy)-1-phenylethyl)piperazine derivatives. The compounds are neurokinin 1 (NK1) receptor antagonist and/or serotonin reuptake inhibitors, with medical indications for depression and other disorders
US7151108 Anticarcinogenic, antiproliferative, and antitumor agents A compound selected from those of formula (I): wherein: W1 represents, together with carbon to which it is bonded, phenyl, pyridyl, Z represents a group of formula U—V as defined in the description, Q1 represents oxygen, NR2 as defined in the description, Q2 represents oxygen, NR′2 as defined in the description, X1, X2, X′1 and X′2 each represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y1, Y2, Y′1 and Y′2 each represents hydrogen, or X1 and Y1, X2 and Y2, X′1 and Y′1, X′2 and Y′2 with carbon carrying them, together form carbonyl or thiocarbonyl, R1 is as defined in the description, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.
CA2194885C Substituted benzamidines, their preparation and their use as pharmaceutical compounds The new compounds of formula (See formula I) (the definition of A and R1 to R4 is given in the specification) may be prepared by conventional methods and may be used therapeutically, inter alia, as LTB4-antagonists.
WO2007105823A1 Prophylactic/therapeutic agent for alzheimer's disease The object is to provide a pharmaceutical agent which is effective for the prevention of the occurrence of Alzheimer's disease induced by an intracellular aggregation mechanism. Disclosed is an agent for preventing/treating Alzheimer's disease by inhibiting the intracellular accumulated amyloid β-dependent and/or p53-dependent cell death. The agent comprising apomorphine hydrochloride as an active ingredient. The action of the agent relies on the prevention of the aggregation/deposition of an amyloid β protein in a cell and the activation of intracellular proteasome. Therefore, the agent can be used for the definitive treatment of Alzheimer's disease.
US20110268826 GIP-Increase Inhibitor A GIP-increase inhibitor, which is useful as a drug or a food, comprising a rice bran extract as an active ingredient.
US20110071139 Cycloalkyl Lactame Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 This invention relates to novel compounds of the Formula (I), any of the formulas I1-I26 Ia1-3-Ij1-3 or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
WO2010092468A1 Composition comprising alginates and d-limonene to treat gerd and dyspepsia The invention refers to nutritional and pharmaceutical compositions for the use in the treatment and relief of GERD and dyspepsia in mammals, including humans The compositions comprise a combination of alginates of low and high molecular weight and d-limonene in microdispersed form. This combination can be further improved with an antacid or an essential oil with high cholinesterase inhibitory activity.
WO2013154109A1 Novel 1-substituted indazole derivative Provided is a therapeutic drug for diseases associated with central nervous system (CNS) and/or peripheral nervous system (PNS) cholinergicity, diseases associated with smooth muscle contraction, endocrine diseases, diseases associated with neurodegeneration, and the like, said therapeutic drug having strong α7 nicotinic acetylcholine receptor (α7 nAChR)-regulating activity and that contains a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. [In formula (I), A is CR1E or a nitrogen atom, X-Y-Z is N-CO-NR3AR3B, or the like, R1A through R1E are the same or different and represent hydrogen atoms, or the like, R2A through R2D are the same or different and represent hydrogen atoms, or the like, R3A and R3B are the same or different and represent optionally substituted C3-10 cycloalkyls, or the like, and n is 1 or 2.]
EP1692116B1 1,2,3-triazole amide derivatives as inhibitors of cytokine production Disclosed are compounds of formula (I), where Ar1, X, R3, R4, R5 and R6 are defined herein. The compounds of the invention inhibit production of cytokines and are thus useful for treating cytokine mediated diseases. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
US20120263795 Aqueous suspensions of submicron 9-hydroxyrisperidone fatty acid esters The present invention is concerned with a pharmaceutical composition suitable as a depot formulation for administration via intramuscular or subcutaneous injection, comprising: (1) as an active ingredient a therapeutically effective amount of a 9-hydroxy-risperidone fatty acid ester or a salt, or a stereoisomer or a stereoisomeric mixture thereof in submicron form and (2) a pharmaceutically acceptable carrier; wherein the pharmaceutically acceptable carrier is water and the active ingredient is suspended therein: and with a process of preparing such a composition. The invention further concerns such a pharmaceutical composition for use as a medicament in the treatment of psychosis, schizophrenia, schizoaffective disorders, non-schizophrenic psychoses, behavioural disturbances associated with neurodegenerative disorders, e.g. in dementia, behavioural disturbances in mental retardation and autism, Tourette's syndrome, bipolar mania, depression, anxiety.
US20110288004 Viral Sequences and Uses Thereof The invention features polypeptide and polynucleotide sequences based on the 134R sequence. In some embodiments, these sequences include a heterologous signal sequence, such as the myxoma virus T7 signal sequence. The invention also features methods for treating immunological disorders and neoplasms (e.g., cancer) using the polypeptides and nucleotides described herein. Finally, the invention features fusion proteins including the myxoma virus T7 signal sequence.
CN1628693A Glossy ganoderma preparation containing main active substance of glossy ganoderma herb and preparing method thereof The invention discloses a glossy ganoderma preparation containing main active substance of glossy ganoderma herb and preparing method, wherein each 100g of the ganoderma spore powder preparation comprises glossy ganoderma polysaccharides 10-50g, triterpene 3-10g, nucleosides 2-6g, amino acid 10-25g, the glossy ganoderma polysaccharide comprises polysaccharide in glossy ganoderma spore powder and polysaccharide in glossy ganoderma fruiting body by the weight ratio of 1/9-9/1.
CN101591341A Alkyl porphyrin compound, preparation and application thereof in field of medicaments and pesticides The invention relates to an alkyl porphyrin compound. A chemical structural formula is shown as the right, wherein R1 is an alkyl, naphthenic base or heteroatom-containing naphthenic base; R2 is an alkyl, naphthenic base or heteroatom-containing naphthenic base; R1 and R2 are same or different; and the alkyl porphyrin is a pureple solid, and can be decomposed at a melting point of over 300 DEG C. The preparation comprises the following steps of: using pyrrole and 6-chlorine-1-hexanal as raw materials; under the action of Lewis acid, adding tetrachlorobenzoquinone for oxidation and organizing; preparing an important intermediate of 5,10,15,20-tetra-(5-amyl chloride)-porphin; performing the displacement reaction of the intermediate and different bisacetamidt; eluting the residuals by silica gel column chromatography; and collecting the product. The alkyl porphyrin compound has good fat solubility and water solubility, high selective absorption in a tumor cell, so that the compound is an ideal photosensitizer; and the synthetic route has the advantages of simple operation, low cost, environmental protection and good economic benefits and application prospect.
CN101336912A Eye in-situ gel of compound taurine The invention discloses a compound taurine eye gel and a preparation method thereof. The compound taurine eye gel contains (per 1,000 mL) taurine 10 g, chlorphenamine maleate 100 mg, L-potassium aspartate 2 g, aminocaproic acid 10 g, antiseptic 0.05-1 g, osmotic pressure regulator 1.0-7.5 g, gel matrix 30-150 g, and acid/base buffer and water for injection in balancing amount. The inventive compound taurine eye gel optimizes adjuvants and improves production process, so as to enrich the compound taurine dosage forms, remarkably prolong the retention time of the compound taurine in eyes, and improve the therapeutic effect; and has no adverse irritant reactions.
WO2011121150A1 Enteral or oral food product intended, in particular, for nutrition and for the prevention and improvement of neurological alterations, neurodegenerative alterations or cognitive disorders The invention relates to a complete food product for specific nutritional use that is intended, in particular, for enteral or oral nutrition in the case of patients with neurological or neurodegenerative alterations, as well for the prevention of states of cognitive or behavioural deterioration, particularly in the elderly. The food product comprises: a functional ingredient that has been specially formulated for the nutrition of patients suffering from or likely to develop neurological or neurodegenerative alterations, cognitive deterioration or behavioural disorders; a carbohydrate mixture; a protein mixture; a lipid mixture; as well as dietary fibre, inulin, vitamins and minerals.
CN103356533A Application of Sarcaboside A in medicine for inhibiting liver fibroblast proliferation The invention discloses an application of Sarcaboside A in preparing a medicine for treating liver fibrosis. Pharmacological tests prove that the Sarcaboside A can obviously inhibit the generation and development of liver fibrosis and can be used for preparing a medicine for resisting liver fibrosis and treating liver cirrhosis. The application of the Sarcaboside A in preparing a medicine for inhibiting liver fibroblast proliferation is revealed for the first time; since a brand new skeleton type is adopted and the activity in inhibiting liver fibroblast proliferation is unexpectedly strong, the possibility of other compounds giving any prompt is avoided, and the Sarcaboside A has outstanding substantive features; and a remarkable progress is made in applying the Sarcaboside A to the resistance against liver fibroblast proliferation.
CN101843631B Application of baicalin in resisting and preventing bacterial infection The invention relates to application of baicalin in resisting and preventing bacterial infection and provides application of baicalin which does not bring survival pressure to bacteria and has little probability of generating resistance to drugs in resisting and preventing bacterial infection.
EP1680132A2 Methods of using and compositions comprising thalidomide for treatment, modification and management of fibromyalgia Methods of treating, preventing, modifying and/or managing fibromyalgia and related conditions are disclosed. Specific embodiments encompass the administration of thalidomide, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent and/or physical ox psychological therapy. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in the methods of the invention are also disclosed.
EP2024335A1 Novel imidazole derivatives, preparation and user thereof as medicine The invention concerns novel imidazole derivatives of general formula (I), wherein Z' and Z represent different variable groups. Said products have an antitumoral activity. The invention also concerns pharmaceutical compositions containing said products and their use for preparing an antitumoral medicine.
US20110060029 Method of treating cancer by modulating epac Methods of treating cancer by preventing, mitigating, and/or inhibiting cancer metastasis in tumors expressing Epac by inhibiting the activity of exchange proteins directly activated by cyclic AMP (Epac) or one or more proteins within the Epac-induced carcinoma migration pathway.
EP0770140B1 Composition containing nucleic acids and cationic polymers, preparation and uses Compositions containing one or more nucleic acids and cationic polymers, and their use in gene therapy, particularly for in vivo nucleic acid transfer.
CA2608072A1 Aminopiperidine quinolines and their azaisosteric analogues with antibacterial activity The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans.
WO2010012396A1 5,6 substituted benzamide derivatives as modulators of the ep2 receptor The present invention relates to 5,6 substituted benzamide derivatives of the general formula (I), to processes for preparation thereof and to the use thereof for production of pharmaceutical compositions for treatment of disorders and indications connected with the EP2 receptor.
CN101935319A Berberine organic acid salt, berberine organic acid salt inclusion compound and preparation methods thereof The invention provides a berberine organic acid salt, a berberine organic acid salt inclusion compound and preparations method thereof. The berberine organic acid salt consists of an alkali base and a salt ligand, wherein the alkali base is a jamaicin alkali base; the salt ligand is an acid radical of organic acid; the mole ratio of the alkali base to the acid radical of organic acid is 1:1; and the berberine organic acid salt inclusion compound consists of an inclusion base material and the berberine organic acid salt. The method for preparing the berberine organic acid salt comprises the following steps of: neutralizing solution of jamaicin and solution of organic acid into salt; crystallizing the salt; and filtering, leaching and drying the crystallized salt so as to obtain the berberine organic acid salt. The method for preparing the berberine organic acid salt inclusion compound comprises the following steps of: dissolving the inclusion base material; adding the berberine organic acid salt into the dissolved inclusion base material for dissolving and inclusion; cooling and standing reaction liquid to separate coprecipitate out; leaching the coprecipitate with acetone; and drying a filter cake so as to obtain the berberine organic acid salt inclusion compound. The berberine organic acid salt and the berberine organic acid salt inclusion compound provided by the invention have the advantages of high bioactivity, small dosage and high dissolubility. The preparation methods have the advantages of simple process, high product purity, easy operation control, simple equipment and easy realization of industrialized production.
WO2011086307A1 Pyrrolopyridine derivatives as nurr1 activators useful for treating parkinson's disease The present invention relates to a compound of formula (I), where R1, R2, R3, and n are such as defined in the description. The compounds of formula (I) are Nurr1 receptor activators.
WO2010143582A1 Phenylcyclopropylamine derivatives and lsd1 inhibitors Disclosed are compounds capable of selectively inhibiting the function of LSD1 and LSD1 inhibitors. A phenylcyclopropylamine derivative characterized by comprising a compound represented by general formula (I) or (II), a pharmaceutically acceptable salt, hydrate or solvate thereof, or a prodrug of the same. In general formulae (I) and (II), R1 represents hydrogen, or an alkyl group, a phenyl group or a heterocyclic group, each optionally having a substituent attached thereto; R2 represents an alkylene group which is optionally branched and optionally has a substituent attached thereto; R3 represents an alkyl group, a phenyl group, a heterocyclic group or a benzyl group, each optionally having a substituent attached thereto; R4 represents an alkyl group optionally having a substituent attached thereto, a phenyl group optionally having a substituent attached thereto, a heterocyclic group optionally having a substituent attached thereto, an alkyloxy group optionally having a substituent attached thereto, a phenyloxy group optionally having a substituent attached thereto, an alkylamino group optionally having a substituent attached thereto or a phenylamino group optionally having a substituent attached thereto; and X represents O, NH2, NHCO, CONH, S or CH2.
WO2010065755A1 Deuterated pyridinones This invention relates to novel substituted pyridinones, their deuterium-modified derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a TNF (tumor necrosis factor) alpha production inhibitor/TGF (transforming growth factor) beta inhibitor.
CN102861009A Application of L-ascorbic acid in preparation of drug having antagonistic action on cytotoxicity effect caused by cyanea capillata toxin The invention belongs to the technical field of medicines and particularly relates to application of L-ascorbic acid in preparation of drug having antagonistic action on cytotoxicity effect caused by cyanea capillata toxin. In two terms of isolated red blood cell and whole animal the L-ascorbic acid is proven to have antagonistic action on cytotoxicity effect caused by cyanea capillata toxin. An effective alternate medicine is provided for developing medicines for preventing or treating stings of cyanea capillata.
US20110015249 Methods and compositions for treatment of cancer and other angiogenesis-related diseases The present invention provides nucleic acid molecules that modulate the expression of molecules in the angiopoietin/Tie2 signaling pathway. Methods of using the nucleic acid molecules are also provided.
CN103212076A Compositions comprising ceftaroline and methods of treatment The present invention provides compositions comprising ceftaroline or a pharmaceutically acceptable salt, solvate or a prodrug thereof alone or in combination with an antibacterial agent. The present invention provides methods of treating bacterial infection, which include administering an effective amount of ceftaroline or a pharmaceutically acceptable salt, solvate or a prodrug thereof alone or in combination with an antibacterial agent.
US20090221542 Inhibition of Inflammatory Cytokine Production With Tanshinones Provided are methods of attenuating release of a proinflammatory cytokine from a mammalian cell. Also provided are methods of inhibiting or treating an inflammatory cytokine cascade in a mammal. Further provided are methods of treating a mammal at risk for or undergoing sepsis, septicemia, and/or endotoxic shock. Additionally provided are methods of attenuating NO release from a mammalian cell. Also provided are methods of attenuating NO production in a mammal at risk for, or having, a disorder mediated by excessive NO production.
EP2077120A2 Rheumatoid arthritis remedy containing il-6 antagonist as active ingredient There is provided a synovial cell growth inhibitor, or a pharmaceutical composition for treatment of chronic rheumatoid arthritis based on the synovial cell growth inhibitor. The pharmaceutical composition for treatment of chronic rheumatoid arthritis or synovial cell growth inhibitor contains an IL-6 antagonist, such as IL-6 antibody or IL-6R antibody, as an effective component.
EP1614414A2 Compositions comprising a copper compound for treatment of mammalian diseases A composition for use in the treatment of mammalian diseases, such as cancers, viral diseases, protozoan-borne diseases such as malaria, and bacterial diseases, is provided. The composition comprises a core containing a biologically active copper compound, and a sheath, and may include other components such as iron. Methods of making the composition are also provided.
CN103288587A Preparation method of perfluoroalkane The invention provides a method for preparing perfluoroalkane. The method comprises the following steps of: filling a filler in a reactor, fluorating by using a fluorating agent, keeping the temperature inside the reactor between 100 to 300 DEG C, adding reaction materials in a vaporizer to vaporize, controlling the temperature inside the vaporizer between 130 to 150 DEG C, wherein the reaction materials comprise C5-C16 alkanes and one or more of partial fluorides of the C5-C16 alkanes, continuously bringing reaction material vapor in the reactor by using an inert gas, continuously feeding the fluorating agent in the reactor to react with the reaction material vapor continuously fed in the reactor, and separating and purifying to obtain the perfluoroalkane. The method provided by the invention is suitable for large-scale continuous productions; the reaction conditions are easily controlled; the yield is high; the by-products are less; the reaction production is easily separated and purified; no three wastes are discharged during the production process. With the adoption of the method, perfluorooctane with the purity being greater than or equal to 98% can be prepared and can act as a production material of lung cavity ventilation aerating liquid and a preparation for ophthalmologic operations.
EP2601847A1 A nutraceutical compound for treating excess of weight A nutraceutical compound for treating excess of weight comprising a first component comprising a first active ingredient defined by betulin and suitable to regulate the absorption and metabolism of carbohydrates and lipids and a second comprising a second active ingredient defined by 1-deoxynojirimycin, said active ingredient being suitable to control glycaemic metabolism.
CN1931147A Chewing gum containing disease treating component The present invention relates to food technology, and is one kind of chewing gum with disease treating component. The chewing gum has soluble chitosan in 15-25 wt%, except common components, including polymer gum, sweetener, essence, seasoning, etc. Chitosan possesses functions of diminishing inflammation, arresting bleeding and raising the immunity of local cells as well as obvious curative effect on caries, periodontal disease and other oral diseases, so that the chewing gum with chitosan has both physical health and medicinal effects.
CN102048886A Method for preparing lotus root alum powder The invention relates to a method for preparing lotus root alum powder, which comprises the following steps of: firstly, adding XanThium sibiricum leaves, saururus chinensis and towel gourd vine into water for decocting; filtering decoction and removing slag; drying; scraping off lotus root black skin; placing alum into an iron pot and firing the alum on the fire until the alum is dry; and grinding the alum and the medicines into fine powder for later use. The product has an obvious effect for treating chronic sinusitis and nasal polyps which cannot be healed for a short time.
US20100178291 Pyrrolidinone, Pyrrolidine-2, 5-Dione, Pyrrolidine and Thiosuccinimide Derivatives, Compositions and Methods for Treatment of Cancer The present invention relates to pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosucciniroide compounds of formulae (I)-(IV), and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide compound of the present invention.
CN103301447A Application of DNA (Deoxyribonucleic Acid)-PKcs in preparation of medicine for changing drug resistance of tumor cells on MTX (Methotrexate) The invention relates to application of DNA (Deoxyribonucleic Acid)-PKcs in preparation of a medicine for influencing dihydrofolate reductase (DHFR) gene amplification and changing the drug resistance of tumor cells on MTX (Methotrexate) and belongs to biological medicines. The application comprises the following steps: establishing an MTX drug-resistant cell evolution model, selecting low-concentration drug-resistant (HSRs) and high-concentration drug-resistant (DMs) cells as research objects, detecting the gene amplification degree and form in the parent cells and drug-resistant cells, the DNA damage conditions and DNA-PKcs expression conditions, establishing clone which stably interferes the DNA-PKcs in the MTX drug-resistant cells aiming at the core protein DNA-PKcs in the NHEJ path, and detecting the amplification degree and form of DHFR genes in stable interference clone, the cell growth and apoptosis and change of the drug resistance.
WO2007050697A2 Compositions and methods for the administration psychotropic drugs which modulate body weight Embodiments of the invention describe compositions and methods for the administration of fast disintegrating atypical antipsychotics, metabolites of atypical antipsychotics, and antidepressants which reduce weight in patients previously taking conventional formulation of atypical antipsychotics and antidepressants. In a preferred embodiment said fast dissolving atypical antipsychotic is FAZACLO. In another preferred embodiment said fast dissolving metabolite of an atypical antipsychotic is desmethyl clozapine. In another preferred embodiment said fast dissolving antidepressant is paroxetine.
WO2010019611A2 Bridged polycyclic compound based compositions for topical and oral applications A pharmaceutically active agent, a pharmaceutically active agent carrier and method of use thereof are described. In some embodiments, a system may include a composition. The composition may include one or more bridged polycyclic compounds. At least one of the bridged polycyclic compounds may include at least two cyclic groups, and at least two pharmaceutically active agents may be associated with the bridged polycyclic compound. In some embodiments, one or more bridged polycyclic compounds may be applied to an oral surface, topical surface, and/or an otic surface of an animal (e.g., canine, feline) or a human such that an associated malady may be inhibited and/or ameliorated.
US8501240 Compositions comprising an active agent The present invention provides a highly dispersible formulation comprising an active agent and a dipeptide or tripeptide comprising at least two leucyl residues. The composition of the invention possesses superior aerosol properties and is thus preferred for aerosolized administration to the lung. Also provided are a method for (i) increasing the dispersibility of an active-agent containing formulation for administration to the lung, and (ii) delivery of the composition to the lungs of a subject.
EP1513529B1 Triple monoamine reuptake inhibitors for the treatment of chronic pain The present invention relates to the use of triple monoamine reuptake inhibitors for the treatment of chronic pain.
EP1268412B1 Sulphonamido-substituted bridged bicycloalkyl derivatives A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures of formula (I) (where the variables are as defined in the claims). The compounds are inhibitors of η-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
EP2097393A1 Therapeutic g-quadruplex ligands The invention provides compounds of formula (I): wherein Ar1 is a monocyclic aryl or heteroaryl; X and Y are each independe ntly a group of formula (II): Z is absent, a group of formula (II), optionally substituted C1-7 alkyl, optionally substituted C3-20 heterocyclyl, optionally substituted C5-20 aryl, halo, amino, hydroxy, ether, thio, thioet her, carboxy or cyano; L1 and L2 are each independently selected from NR 3, C2H2, CH2, -O-, -S- and a bond; Ar2 and Ar3 are independently optionally substituted C 5 or C6 aryl or heteroaryl; n is an integer from 1 to 5; R1 and R2 are independently hydrog en, C1-7 alkyl, C3-20 heterocyclyl, or C 5-20 aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; R3 is H or C 1-7 alkyl; and provided that at least one of Ar 1, Ar2 and Ar3 is oxazole, triazole or tetrazole. These compounds are thought to bind G -quadruplexes formed in human telomeres and are therefore useful in anti -cancer therapy. The invention also provides pharmaceutical compositions comprising the novel compounds, and methods for their manufacture.
US20080020995 Use of Cyclodextrin Complexes Containing Lipoic Acid The invention relates to the use of cyclodextrin complexes containing lipoic acid, said complexes consisting of at least one representative of the series of unsubstituted α-cyclodextrin, β-cyclodextrin and γ-cyclodextrin, and at least one representative of the series of racemic α-lipoic acid, racemic dihydrolipoic acid and the derivatives thereof, for producing a food supplement, a functional food supplement, a clinical nutrition product and/or a cosmetic preparation in the non-medical field of application. Said complex, which contains at least 20 wt. % of the cyclodextrin component, preferably in food quality, can also contain water and reaction products or secondary reaction products from the complex production, especially α-cyclodextrin being used. The cyclodextrin/(dihydro)liponic acid complexes can be used, preferably combined with other bioactive components, aromas and/or texturing products, and also the standard formulation auxiliary agents, to produce an agent for preventing and/or treating symptoms of an inflammatory nature and especially arthritis, damage to the liver function and especially alcohol intoxication, paraesthesiae and neuropathies, and for producing agents having cytoprotective and/or antiphlogistic and/or antinociceptive (analgesic) properties and/or properties that counteract the formation of radicals. Said complexes can also preferably be used to produce an agent for stimulating glucose metabolism and/or transport in muscles and/or lipocytes, agents for reinforcing the energy metabolism of the body and the brain, agents for increasing the endurance, capacity, attentiveness, concentration of the memory, agents for the prevention and/or treatment of diabetes Typ2, and agents for caring for at least partially keratinised parts of the body, especially the skin, hair, fingernails and toenails. The invention enables products to be obtained, which can be taken by the end consumer under improved compliance conditions in the non-medical field of indication, due to the distinctive stability of the agents.
WO2007068579A1 Biphenyl derivatives as selective agonists of gamma rar receptors The invention concerns novel biphenyl compounds, as well as their use for preparing a pharmaceutical or cosmetic composition for preventing and/or treating pathological conditions for which a selective agonist activity for the gamma subtype of the family of RAR receptors is required.
US20110300086 Film-Forming Solutions Comprising Vitamin D or Derivative Thereof and a Corticosteroid and Dermatological Applications Thereof Topically applicable film-forming solutions, e.g., nail varnishes, useful for such dermatological applications as the prevention or treatment of nail psoriasis, contain, as active agents solubilized therein, vitamin D or derivative thereof and a corticosteroid, formulated into a topically applicable, physiologically acceptable medium therefor.
WO2013078769A1 Conjugate of polyethylene glycol and tamsulosin and pharmaceutical composition thereof Disclosed are a conjugate of polyethylene glycol-tamsulosin as shown in general formula (II) and a pharmaceutical composition containing the conjugate. In the conjugate, P and P' are H or polyethylene glycol but P and P' are not both H simultaneously. Sulfonylamino is contained in the structure of tamsulosin and through an alkylation reaction, low molecular weight polyethylene glycol is introduced into the structure of tamsulosin, reducing the hydrophobicity of tamsulosin, increasing the hydrophilicity thereof, and reducing the blood-brain barrier transmittance thereof, thereby reducing the toxicity thereof.
US7132513 Bifunctional chelating agent The invention concerns a ligand comprising wherein n is an integer from 1 to 5, X represents —NO2, —NH2, —NCS, —NHCOCH2-Z. NHCO—W—COCNHS, —NH-Q, —NHCS-Q, —NHCOCH2-Q, or —NHCO(CH2) m ?-Q where Q is an hapten chosen from the group consisting of steroids, enzymes, proteins, monoclonal antibodies, chimeric antibodies, or fragments thereof or any activated linker ready for coupling reaction, Y is CO2H or PO3H2 W is —(CH2)m— m is an integer from 1 to 10. Z is chloride, bromide or iodine
CN103719328A Panax pseudoginseng health-care tea for treating injure The invention relates to panax pseudoginseng health-care tea for treating injure. The panax pseudoginseng health-care tea for treating injure is prepared by drying 34 g of panax pseudoginseng, 16 g of impatiens balsamina, 17 g of menthol, 17 g of camphor, 15 g of safflower and 16 g of cassia twig in the sun, cutting finely, uniformly mixing with 250 g of green tea and packaging to prepare the finished product panax pseudoginseng health-care tea for treating injure. The panax pseudoginseng health-care tea for treating injure is simple in preparation and sufficient in raw materials, has the efficacy of activating blood, freeing collateral vessels, dissipating stasis and relieving pain, and can help people to improve body recovery capability and alleviate pain and damage caused by injure after brewed and drank.
WO2007140299A3 Use of ixabepilone in combination with cyp3a4 inhibitors for pharmaceuticals Disclosed are Uses of ixabepilone in combination with CYP3A4 inhibitors such as ketoconazole and lapatinib to achieve a surprisingly enhanced pharmacological effect as compared with when ixabepilone is administered unaccompanied by the CYP3A4 inhibitor. Also disclosed are methods of treating cancer in a human patient comprising administering to the human a therapeutically-effective combination of an amount of a the CYP3A4 inhibitor and an amount of ixabepilone to achieve the enhanced pharmacological effect.
WO2011025545A1 Sphingosine type 1 inhibitors and methods for making and using same Provided are novel compositions and analogs which are useful in a number of applications, indications and diseases, as well as for monitoring pharmakinetics and patient management. These compounds and analogs are applicable to treating tumors of the central nervous system, e.g., glioblastoma (GBM).
CN103524590A Diethyl glycyrrhetate and preparation method thereof The invention provides a preparation method of diethyl glycyrrhetate, belonging to the field of organic chemistry. Through a scientific feasible method, mono-ammonium glycyrrhetate used as a raw material is subjected to the steps of esterification, column chromatography, concentration and the like, thus preparing the diethyl glycyrrhetate having favorable lipid solubility and high purity. The diethyl glycyrrhetate can be further prepared into various preparations suitable for clinical application by taking the prepared diethyl glycyrrhetate as a raw material and adding pharmaceutically acceptable auxiliary materials, and the preparations can be used for clinical treatment of liver diseases. The diethyl glycyrrhetate and the preparation method thereof are simple in process, favorable in stability and suitable for industrial production, and have very high practicality.
EP2200584A2 Formulation containing cyclin-dependent kinase inhibiting compound and method of treating tumors using the same This application discloses a novel formulation containing a 3-amino-4-sub stituted pyrazole derivative which has cyclin-dependent kinase inhibiting properties, and a method of treating tumors using the novel formulation.
US20080027125 Fluvastatin sodium novel forms and preparation thereof Provided are a novel solid states of fluvastatin sodium and processes for preparation thereof.
CA2136356C 1,2,3-triazole and imidazole compounds and their antitumor use A discovery underlying this invention is the concordance between particular cellular signaling mechanisms and cancer cell growth and metastasis. It has now been discovered that the compounds inhibit the signal transduction required for the maintenance and driving of the malignant process. These compounds are also effective for the in vivo treatment of solid tumors and related disease states. This invention provides uses for the compounds to inhibit invasion and metastasis of solid tumors, and for the treatment of diseases involving aberrant signal transduction pathways.
US20090221628 Compositions and methods for treatment of prostate and breast cancer Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods of treating specific types of cancer such as prostate, esophageal, glioblastoma, gliosarcoma, NSCLC, head and neck, and breast with the compounds described herein alone and in combination with antineoplastic agents.
WO2011007091A1 Derivatives of 5,6-bisaryl-2-pyridine-carboxamide, preparation thereof, and therapeutic use thereof as urotensin-ii receptor antagonists The present invention relates to compounds of formula (I), where: A is a (C-1-C4)alkyl group; W is a halogen atom; E is a CR3 member where R3 is a halogen atom or a hydrogen atom, or E is a nitrogen atom; B is a -NR1 R2 group where Ri is a hydrogen atom or a (C-1-C4)alkyl and R2 is a (C1-C4)alkyl group; V is a hydrogen atom, a halogen atom, or a (C1-C4)alkyl group; Z is an oxygen atom or a -CH2- group; or to the acid or base addition salt thereof. The invention also relates to a method for preparing same and to the therapeutic use thereof.
WO2014080703A1 Modified galectin-9 protein Provided is a modified form of galectin-9, which has substantially the same physiological activity as that of wild-type galectin-9, also has excellent protease stability and solubility, and can be produced with high yield. The modified form of galectin-9 according to the present invention is a protein which comprises a NCRD and a CCRD as mentioned below, wherein each of the NCRD and the CCRD comprises an N-terminal domain and a C-terminal domain, and wherein the C-terminal of the NCRD and the N-terminal of the CCRD are bound to each other directly or indirectly. The NCRD is (N1) a peptide comprising the amino acid sequence represented by SEQ ID NO: 1. The N-terminal domain of the CCRD is (C-N1) a peptide comprising an amino acid sequence produced by deleting 1 to 17 amino acid residues in the amino acid sequence represented by SEQ ID NO: 3, and the C-terminal domain of the CCRD is (C-C1) a peptide comprising the amino acid sequence represented by SEQ ID NO: 5.
CN102600122A Paster for treating dental ulcer and preparation method thereof The invention aims to provide a paster for treating dental ulcer and a preparation method thereof. Aiming at the defects of the existing dental ulcer preparation, the oral paster containing L-glutamine and sodium azulenesulfonate has the advantages of simple preparation process, stable drug release, durable action to ulcer position and remarkable curative effect.
EP1731161A1 Compositions for the treatment of diseases associated with elevated sphingolipid concentrations Methods and compositions are disclosed that are useful for the prevention and/or treatment of cardiovascular and cardiac diseases and disorders, or damage resulting from surgical or medical procedures that may cuase ischemic or ischemic/reperfusion damage in humans; and cardiovascular trauma. The beneficial effects of the compositions and methods are achieved through the use of pharmaceutical compositions that include agents that interfere with the production and/or biological activities of sphingolipids and their metabolites, particularly sphingosine (SPH) and sphingosine-1-phosphate (S-1-P). Also disclosed are methods for identifying and isolating therapeutic agents.
WO2014093606A1 Pyridone derivatives and uses thereof in the treatment of tuberculosis A compound of Formula (I) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the inhibition of mycolic acid biosynthesis through inhibition of M. tuberculosis EnoyI Acyl Carrier Protein Reductase enzyme (InhA): wherein R1, R2, R3, R4 and R5 are as defined herein.
EP1704136B1 Gossypol derivatives, production method thereof and uses of same The invention relates to compounds having general formula (I), wherein R1 and R2 represent, independently of each other, -OH, or -CH2-O-R3, or -CH2-S-R3, or formula (II), R3, R4, R5 and R6 representing, independently of each other, -H or a carbon group with between 1 and 10 saturated or unsaturated carbon atoms optionally substituted by one or more heteroaromatic groups. The invention also relates to pharmaceutical compositions that contain said compounds and to the uses thereof, including for the treatment of cancers.
EP2044062A1 Indole compounds Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein X, R1,R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
CN102058603A Disubstituted zinc phthalocyanine composite, and preparation method and application thereof The invention discloses a new medicine for treating cancers or precancerous lesions by utilizing a photodynamic therapy, and the medicine provided by the invention contains 4 zinc phthalocyanine isomer composites. The invention simultaneously provides the industrial chromatograph preparation process of the medicine. The preparation method provided by the invention comprises the following steps: separating 10 cis-isomers from the synthetic bisulfo biphthalyl dicarboximide zinc phthalocyanine; and further separating 4 isomers with better amphipathy from the synthetic bisulfo biphthalyl dicarboximide zinc phthalocyanine. The experiment indicates that the properties of the composite provided by the invention are superior to the mixture containing the 10 cis-isomers.
US7737142 (Thio) carbamoyl-cyclohexane derivatives as D3/D2 receptor antagonists The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may form a heterocyclic ring with the adjacent nitrogen atom; X represents an oxygen or sulphur atom; n is an integer of from 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine receptors.
US20110014275 Compositions and methods for inhibiting or inducing adipogenesis This invention relates generally to compositions and methods which utilization nuclear receptors for regulating adipogenesis in cells. Specifically, the invention is directed to compositions which regulate transcription factor PPARγ, and enhance or inhibit the transcription of genes responsible for directing cell differentiation towards a pathway of adipogenesis. More specifically, disclosed herein is a novel polypeptide coactivator of PPARγ, and fragments thereof, which possess coactivator or corepressor activity. Also related are nucleotide sequences which express these polypeptides. Also disclosed is an interfering RNA that may be used to inhibit adipogenesis.
CN103054878A Application of alisol A23-acetic acid ester for preparing medicine for treating hyperlipidemia The invention discloses a novel purpose of alisol A23-acetic acid ester, and discloses an application of alisol A23-acetic acid ester for preparing a medicine for treating hyperlipidemia. Found by animal experiments and researches, the alisol A23-acetic acid ester can be used for preparing the medicine for treating hyperlipidemia, and can treat cardiovascular diseases such as atherosclerotic and fatty liver caused by hyperlipidemia. long-term usage of the alisol A23-acetic acid ester can obviously reduce the rising of large mice transaminase (AST, ALT) due to feeding of a high-fat diet, and the alisol A23-acetic acid ester can display good liver protecting effect. Compared with hypolipemic medicines such as simvastatin and fenofibrate on the market, the alisol A23-acetic acid ester is suitable for long-term usage.
EP2209450A1 Slow release of organic salts of local anesthetics for pain relief Particles of an organic acid salt of an amino acid amide or ester local anesthetic are employed as agents for the improved alleviation of pain. Particularly, the particles find use with surgically created wounds, where the particles may be administered directly into the bed of the wound or topically for transdermal transport.
US6841551 Administering substance P receptor antagonist selected from the group consisting of L 742694, L 758298, and LY 303241, a non-toxic magnesium compound and a pharmaceutically acceptable vehicle A treatment for brain, spinal and nerve injury comprising use of a substance P receptor antagonist optionally in combination with a magnesium compound. There is also provided a formulation for use in this treatment comprising a substance P receptor antagonist and a magnesium compound.
US20080226747 Cell proliferation; anticancer agents; bioavailability The present invention relates to pharmaceutical formulations comprising the protein kinase inhibitor, MP470, and methods of using same in treating conditions involving undesirable cell proliferation, such as cancer.
US20050020541 Moderate neurotransmitters A compound of formula (I): wherein R1 and R2 are, independently, hydrogen or alkyl or together, with the nitrogen atom, form a heterocyclyl; R3 and R4 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halogen or trifluoromethyl; R5 is hydrogen or alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof or a prodrug form that is hydrolysable to a compound as defined above.
US20120219561 Prophylaxis Against Cancer Metastasis This document provides prophylactic methods for reducing cancer metastasis by targeting LCN2, MMP9, and CX-CR4.
US20080089876 Composition Containing Statins and Omega-3 Fatty Acids A combination is described comprising at least one omega-3 fatty acid, optionally esterified or salified, at least one statin, Coenzyme Q10, resveratrol, at least one policosanol, pantethine, selenium, and zinc. This combination is endowed with a synergistic effect and is useful in the treatment of disease forms due to insulin resistance and in cardiovascular diseases.
CN101407506A Benzofuran derivatives and uses thereof The invention provides a benzo furan derivative, the molecular structure of which is as shown in formula I. The compound is firstly isolated from (Lespedeza virgata (Thurb) DC), the molecular formula is C18H16O7, the molecular weight is 344, and the compound is greenish black random powder at normal temperature and normal pressure. Experiments show that the compound has functions of treating nephritis and anti-oxidation, and the compound can be used for preparing medicines for treating nephritis.
US7915232 4′-substituted nucleoside derivatives as inhibitors of HCV RNA replication The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof which inhibit HCV polymerase and are useful for treating a patient suffering from a HCV infection and to pharmaceutical compositions containing such compounds.
US8017605 P38 kinase inhibiting agents Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
WO2013130407A1 Small molecule inhibitors of p-type atpases Small, low molecular weight compounds of the formula I and/or the formula II, as defined herein, which inhibit Cu-ATPases, ATP7A and ATP7B. Compositions and methods therefore, are provided.
US20090181976 Use of Compounds Binding to the Sigma Receptor for the Treatment of Metabolic Syndrome The present invention refers to the use of compounds binding to the sigma receptor for the treatment of metabolic syndrome.
EP1261347B1 Therapeutic compositions and methods for treating periodontitis with antiinflamatory compounds Methods of promoting healing through enhanced regeneration of tissue (e.g. hard tissue or soft tissue) by contacting the tissue or the surrounding tissue with an anti-inflammatory agent. These methods are useful in a variety of dental and orthopedic applications.
CN1895520A Gastrin magnesium granules and preparation thereof A medicine 'Gastric bismuth magnesium particle' and its preparing process are also disclosed. It features that the volatile oil of grass-leaved sweetflag rhizome is wrapped by beta-cyclodextrin, and its additive (sweetening agent and tangerine essence) is carefully chosen.
US20100104620 Over-coated product including tableted center and medicament Methods and products for delivering a medicament or agent to an individual are provided as well as methods for producing the product. The product includes a coating having a medicament or agent. The medicament or agent is present within the coating that surrounds a tableted center. The tableted center is defined by compressible excipients. By chewing the product, the medicament or agent is released from the product within the buccal cavity.
US20080063701 Lipids of a liposome comprising cationic N1-cholesteryloxycarbonyl-3,7-diazanononane-1,9-diamine and/or noncationic dioleoyl phosphatidylethanolamine and short interference RNA (siRNA) are coupled, reversibly or irreversibly, to one or more polymers; drug delivery; freeze drying The present invention relates to a non-viral delivery vector comprising a liposome, wherein one or more lipids of the liposome are coupled, reversibly or irreversibly, to one or more polymers, and wherein the liposome comprises siRNA.
CN101805762A Purpose of separating arabinose through candida tropicalis fermentation and pharmaceutical and health care purposes of high-purity arabinose separation product The invention relates to a purpose of candida tropicalis, a microbial fermentation and a separation preparation method for separating arabinose through yeast, and pharmaceutical and health care purposes of a high-purity arabinose separation product prepared by the method. The arabinose of the invention has high output quality and high yield, and the product is applied to pharmaceutical and food fields.
US20100292200 Methods for Modulating Apoptosis in Platelets The description discloses methods of enhancing or maintaining the viability or lifespan of platelets comprising administering an agent that down modulates apoptosis. The description also discloses a method of decreasing the survival, lifespan or viability of platelets comprising administering an effective amount of an agent that enhances apoptosis.
EP1569650B1 Use of levocetirizine for the treatment of persistent allergic rhinitis The present invention relates to a pharmaceutical use of levocetirizine for the treatment of persistent allergic rhinitis.
WO2009133348A1 Aminopyridine derivatives The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (such as asthma or COPD); and methods of treating patients with such compounds; wherein R1 - R11 are as defined herein.
US20080311200 Controlled Slow Release Formulation of Thiamine and Use Thereof in the Treatment of Pathologies Connected to Defective Process of Learning and Memorization The present invention relates to thiamine controlled-release pharmaceutical compositions and their use in medicine for resolving absorption defects or deficiencies of thiamine itself from the organism. Said compositions have revealed to be useful in the treatment of cerebral pathologies connected with learning and memorizing processes. In particular, said compositions have revealed to be useful in the treatment of the Alzheimer's pathology, preferably in the forms of slight-medium intensity.
US20060083790 Combination of an ibat inhibitor and a metal salt for the treatment of diarrhoea A combination comprising an IBAT inhibitor, or a pharmaceutically acceptable salt, solvate of such a salt or a prodrug thereof, and a metal salt, wherein the metal salt is formulated to release in the terminal ileum, caecum and/or the colon, is described. Compositions containing this combination and uses of the combination are also described.
WO2010031265A1 Pharmaceutical composition for the treatment of proliferative diseases The present invention provides a pharmaceutical composition for the treatment of proliferative diseases, such as tumor, wherein the pharmaceutical composition contains a compound of formula (I) or its pharmaceutically acceptable salts and at least one antiproliferative medicament. The pharmaceutical composition has a synergistically increased action.
WO2006088310A1 A pharmaceutical composition comprising retinoid for prevention and treatment of vitiligo The present invention relates to a pharmaceutical composition for the prevention and treatment of vitiligo comprising retinoid as an effective ingredient, precisely a pharmaceutical composition for the prevention and treatment of vitiligo designed to effectively work for vitiligo caused by apoptosis or necrosis of melanocytes by increasing the cell density by reducing apoptosis of human keratinocytes. The pharmaceutical composition of the invention containing retinoid as an effective ingredient not only prevents skin atrophy caused by corticosteroid, a conventional treatment agent of vitiligo, but also inhibits apoptosis of melanocytes and thus improving pigmentation, so that it can be effectively used for the prevention and treatment of vitiligo.
CN103054806A Alvimopan solid dispersion and preparation method thereof The invention relates to an alvimopan solid dispersion and a preparation method thereof. The alvimopan solid dispersion comprises medicinal alvimopan and a carrier, wherein the carrier is a hydrophilic macromolecular carrier, and the weight ratio of the medicinal alvimopan to the hydrophilic macromolecular carrier is 1: (1-9). The alvimopan solid dispersion has improved water solubility, the dissolution rate of the medicament is improved, the gastrointestinal absorption is promoted, and the bioavailability is improved.
US20080306030 Use of a TRPM5 Inhibitor to Regulate Insulin and GLP-1 Release The present invention is directed to methods of enhancing insulin release, GLP-1 release, and insulin sensitivity, methods of increasing insulin gene expression, methods of decreasing gastric secretion and emptying and glucagons secretion, and methods of inhibiting food intake, and methods of treating diabetes mellitus, insulin resistance syndrome, hyperglycemia, and obesity comprising administering to a subject an effective amount of a TRPM5 inhibitor.
US20110077214 Method for treating hyponatremia employing an sglt2 inhibitor and composition containing same Methods are provided for treating hyponatremia, employing an SGLT2 inhibitor alone, or in combination with a supply of carbohydrate, and/or in combination with a diuretic agent. Additionally, compositions comprising an SGLT2 inhibitor optionally with a supply of carbohydrate, and/or a combination of an SGLT2 inhibitor and a diuretic agent are provided in the instant invention and are provided for use in the inventive methods.
WO2009071753A1 4-phenyl-1,3-thiazole and 4-phenyl-1,3-oxazole derivatives as cannabinoid receptor ligands The invention relates to novel 4-phenyl-1,3-azole derivatives of general formula (I) in which R1, R2, R3, R4, X, A, B and n are variable, in a racemic or enantiomer form or any combinations of these forms. These compounds have an affinity for cannabinoid receptors and can therefore be used as medicaments for treating or preventing pathological states and diseases in which one or more of these receptors is (are) involved. The invention also relates to pharmaceutical compositions containing said products and the use thereof for the production of a medicament.
US6849636 Useful for treatment of noninsulin-dependent diabetes, hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
US20090069357 Deuterium-enriched iclaprim The present application describes deuterium-enriched iclaprim, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20100330187 Capsicum food additive and uses thereof The invention relates to a food additive that includes, relative to the total weight thereof: about 3.5 wt % of capsicum oleoresin containing 6 wt % of a capsaicine and dihydrocapsaicine mixture; about 5.5 wt % of cinnamaldehyde; about 9.5 wt % of eugenol; the balance up to 100% consisting of hydrogenated vegetable oils. The invention also relates to the uses of said additive for improving the daily distribution of food ingestion by animals, for increasing the amount of water drunk by animals, or for preparing a food product intended for the preventive or therapeutic treatment of animal digestive disorders, such as acidosis or bloating. This food additive is particularly adapted for ruminants such as bovine cattle.
EP1169327B1 L-arabino-disaccharides of anthracyclines, processes for their preparation, and pharmaceutical compositions containing them The present invention refers to compounds of general formula (I), the pharmaceutically acceptable salts thereof, the processes for their preparation, and the pharmaceutical compositions containing them.
WO2009150331A1 Novel azabicyclic derivatives, preparation method for same, and pharmaceutical compositions containing same The invention relates to compounds of Formula (I): where: *ALK is an alkylene chain, and *W is a grouping selected from N – η – R or η – N – R R1 O O R1, where R and R’ are as defined in the description. The invention can be used for drugs.
WO2009075610A1 Use of benomyl fungicide as an agent for treating oncological diseases The invention relates to the use of benomyl C14H18N4O3 fungicide as an agent for treating oncological diseases with a single dose of 0.1 mg to 5g three times a day. In particular cases, it is preferable to administer the agent diluted in water or a physiological solution with a ratio ranging from 10-11 to 10-3 mmol/l, the solution can be rectally administered or the 1-10% solution of agent is inhaled, or an agent-based 1-15% ointment is used, or the agent is administered in the form of suppositories, or the 1-5% agent solution is intravenously administered or the agent solution is intramuscularly administered with a single dose ranging from 100 to 200 mg. Thus, the invention discloses the effective medicinal agent which exhibits a wide spectrum of therapeutic modalities with respect to different oncological diseases, is easily accessible, not expensive, non-toxic, devoid of side effects when used in pharmaceutically acceptable doses, and which makes it possible to reduce the length of treatment and increase the effectiveness of treatment.
US8197839 A miniature coated tablet or covered rod implant; smaller size and larger payloads than immediate release tablets; veterinary medicine A sustained release apparatus including at least one sustained release mini tablet implant; the or each mini tablet implant including a pharmaceutically active composition including at least one pharmaceutically active component; and a carrier therefor, wherein the or each tablet implant is of the coated tablet or covered rod type; the or each mini tablet implant being approximately 0.1 to 0.5 times the length and/or diameter of a single immediate release tablet capable of providing the desired threshold blood level depending on the pharmaceutical active selected, and having a payload of approximately 30% to 70% by weight of the total payload of an equivalent immediate release treatment conducted for an equivalent period; the sustained release apparatus providing, in use, zero order release of pharmaceutical active.
EP2348031A2 17-Alpha-substituted-11-beta-substituted-4-aryl and 21-substituted 19-norpregnadienedione as antiprogestational agents The invention provides 17-alpha-substituted-11-beta-substituted-4-aryl and 21-substituted 19-norpregnadienediones as antiprogestational agents.
EP1912937A1 Novel substituted azetidinones Novel azetidinones and pharmaceutical compositions are described, as are the methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis.
US20080187523 Nucleotide sequences coding genetically engineered zinc finger protein for use in treatment and prevention of cell proliferative disorders Disclosed herein are methods and compositions for treatment of conditions requiring inhibition of angiogenesis. Such conditions include those characterized by neovascularization, such as retinopathies, macular degeneration and various malignancies.
EP2630145A1 Carbonate derivatives for the treatment of cough The invention relates to use of certain quinuclidine carbonate derivatives as cough suppressants, particularly for treating patients with upper respiratory tract infections or asthma.
CN101716178B Antitumor medicament The invention discloses an antitumor medicament in the technical field of medicine chemical industry, which refers to 6-substituted-5, 6-dihydropyrrol [3, 4-d] pyridine-7-ketone (IV), having the following structural general formulas. The medicament is a compound with higher protein kinase inhibiting activity, has a simple preparation method and convenient raw material sources, is easy to realize industrialization and can satisfy the requirement for preparing the medicament for clinically treating cancers.
CA2383351C Xanthine derivatives as selective antagonists of a2b adenosine receptors A compound of formula (I), wherein R is an aliphatic or cycloaliphatic amine group or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable salt thereof. The compounds of formula (I) may be used to treat, among other indications, asthma and diarrhea.
US20100069325 Pharmaceutical composition for treatment of chronic liver diseases and use thereof A pharmaceutical composition for treatment of chronic liver diseases, the composition including at least cordyceps sinensis polysaccharide, amygdaloside, and gypenoside. The pharmaceutical composition slows down liver fibrosis, stops the development thereof, or reverses the same. A method of using the pharmaceutical composition for treatment of chronic liver diseases.
WO2010133016A1 Pharmaceutical composition for treating depression, preparation method and use therefor Provided in the present invention are a pharmaceutical composition for treating depression and a preparative method and use therefor. The pharmaceutical composition comprises ginsenoside Rg1, ginsenoside Rb1 and glycyrrhizic acid or glycyrrhetinic acid, and has undergone screening to arrive at the preferred ratio of components. Test-proven, the pharmaceutical composition in the present invention can prevent and treat depression and its complications.
WO2009138601A3 Use of mannose-6-phosphate for controlling angiogenesis, ligament regeneration, and cartilage reconstruction The invention relates to the use of mannose-6-phosphate (M6P) and of certain derivatives thereof for controlling angiogenesis and ligament regeneration and/or cartilage reconstruction. The MP6 and certain derivatives thereof can particularly be used for preparing a pharmaceutical composition used for ligament regeneration and/or cartilage reconstruction.
CN1781491A Treating agent of plant poly pentene alcohol gor liver damage The present invention relates to plant polypentene alcohol preparation for preventing and treating alcoholic liver, fatty liver, liver cancer and other liver damage caused by chemical matter or toxin. The plant polypentene alcohol preparation has plant polypentene alcohol in birch polypentene alcohol structure as medicinal active component. The plant polypentene alcohol in birch polypentene alcohol structure is different from conifer polypentene alcohol or dolichol in structure and chain length, and may be used directly in liver damage treating preparation without needing other synthesis.
WO2003073983A3 Methods and compositions in treating pain using diacylglycerol kinase epsilon The present invention relates to methods for the diagnosis and treatment of pain or painful disorders. Specifically, the present invention identifies the differential expression of 9949, 14230, 760, 62553, 12216, 17719, 41897, 47174, 33408, 10002, 16209, 314, 636, 27410, 33260, 619, 15985, 69112, 2158, 224, 615, 44373, 95431, 22245, 2387, 16658, 55054, 16314, 1613, 1675, 9569 and 13424 genes in tissues relating to pain sensation, relative to their expression in normal, or non-painful disease states, and/or in response to manipulations relevant to pain. The present invention describes methods for the diagnostic evaluation and prognosis of various pain disorders, and for the identification of subjects exhibiting a predisposition to such conditions. The invention also provides methods for identifying a compound capable of modulating pain or painful disorders. The present invention also provides methods for the identification and therapeutic use of compounds as treatments of pain and painful disorders.
CN1762482A Antivirus effervescence tablet The invention relates to an antivirus effervescence tablet wherein the raw materials comprise isatic root, capsule of weeping forsythia, gypsum, anemarrhena rhizome, reed rhizome, dried rehmannia root, patchouli, grassleaved sweetflag rhizome and curcuma aromatica.
US7402601 ADMINISTERING A DRUG CONTAINING N-(4-TRIFLUOROMETHYLphenyl)-5-METHYLISOXAZOLE-4-CARBOXANILIDE or N-(4-TRIFLUOROMETHYLPHENYL)-2-CYANO-3-HYDROXYCROTONAMIDE; antiinflammatory agents, immunomodulators, immunosuppressants The use of compound 1 and/or 2 of the formulae and of physiologically tolerable salts of compound 2 for the treatment of rejection reactions of the organ recipient to the transplanted organ is described.
CN101784278A Purin derivatives for use in the treatment of FAB-related diseases The specification describes the use of selected purine derivatives for the treatment of hyperproliferative diseases.
US7179491 Contacting marine oil with an effective amount of a silica under a vacuum;contacting the oil with an effective amount of a bleaching clay;separating the silica from the oil; and separating the clay from the oil Triglyceride oil derived from marine sources, mammalian and fish, is treated with a silica at relatively low temperature under vacuum and is then further treated with a bleaching clay under vacuum and at higher temperature. The silica and the bleaching clay are then separated from the oil. The oil treated by this method is essentially free of proteinaceous materials, phosphatides and mucilage, pro-oxidant metals and very low in colored compounds, and is suitable for deodorizing. The deodorized oil is completely bland, unchanged in the concentration of the long-chain highly unsaturated fatty acids (EPA, DPA and DHA), very low in color, peroxides and secondary oxidation products, free of pesticides and has very good flavor stability. The method avoids the use of any chemicals, such as in the acid and base treatments required in conventional degumming and alkali refining of oils of marine origin. This avoids the formation of artifacts in the oil and trace contamination with chemicals. It also reduces the number of process steps required to produce deodorized food oil from marine sources, which is advantageous in respect to oil quality, process losses and processing costs. The method is especially environmentally advantageous, since it avoids the need for soapstock and waste water processing entirely. Refined oil produced by the method is useful as a nutritional supplement and in methods of therapy or medical treatment.
EP2040750A2 Methods and compositions for increasing the efficiency of therapeutic antibodies using gamma delta t cell activators The present invention relates to methods and compositions for increasing the efficiency of therapeutic antibodies. More particularly, the invention relates to the use of a therapeutic antibody in combination with a γδ T cell activating compound or activated γδ T cells, thereby allowing a potentiation of γδ T cell cytotoxicity in mammalian subjects in order to enhance the efficiency of the treatment in human subjects, particularly through an increase of the depletion of targeted cells.
CN103211820A Method for preparing tegafur, gimeracil and oteracil potassium capsules The invention relates to a method for preparing tegafur, gimeracil and oteracil potassium capsules. The method comprises the steps of dissolving tegafur in methanol, dissolving gimeracil in a hydrochloric acid solution, dissolving oteracil potassium in a sodium hydroxide solution, rapidly mixing the three solutions, rapidly adding microcrystalline cellulose and stirring, slowly cooling to about 4 DEG C at the same time to obtain nanoscale drug adhered to the microcrystalline cellulose, drying drug-containing particles, adding a lubricant into the dry particles, uniformly mixing and encapsulating. According to the invention, the technologies of acid-base neutralization and nanometer crystallization are creatively utilized to prepare nanoscale tegafur, gimeracil and oteracil potassium, so that the drug dissolution rate is greatly increased.
US20100035925 Compounds, pharmaceutical compositions an dmethods for inhibiting hiv infectivity Compounds that possess anti-infective activity are described. Methods of using these compounds for the treatment or prevention of infectious diseases such as acquired immunodeficiency syndrome (AIDS) are also described. The compounds inhibit HIV infectivity and do not exhibit significant cytotoxicity in HIV producing cells.
US20120329777 Amino-Heterocyclic Compounds The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.
WO2008127591A3 Pyrimidinedione derivatives and use thereof The present invention relates to Pyrimidinedione Derivatives, compositions comprising a Pyrimidinedione Derivative and methods for using the Pyrimidinedione Derivatives for treating or preventing a metabolic disorder, dyslipidemia, a cardiovascular disease, a neurological disorder, a hematological disease, cancer, inflammation, a respiratory disease, a gastroenterological disease, diabetes, a diabetic complicaton, obesity, an obesity-related disorder or non-alcoholic fatty liver disease.
US20110060053 Crystalline Modifications of 6-Dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol Crystalline modifications of (1R,3R,6R)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol, (1S,3S,6S)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol and mixtures thereof, pharmaceutical compositions and medicaments comprising these modifications, the use of these modifications as well as to a process for the enrichment of (1R,3R,6R)- or (1S,3S,6S)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol.
US20120214791 Imidazo[5,1-f][1,2,4]Triazines for the Treatment of Neurological Disorders The present invention relates to compounds of the Formula and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.
US20120220658 Method for Treating Sepsis or Septic Shock The present invention is a method for treating sepsis or septic shock using Lipoxin A4.
US20130012592 Agomelatine hydrobromide hydrate and preparation thereof The present invention relates to an agomelatine hydrobromide hydrate of formula I wherein X is Br, preparation and use thereof, and to pharmaceutical compositions containing it. The agomelatine hydrobromide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps.
EP2168950A1 Inhibitor of the differentiation of t cells into th1 cells The present invention is to provide an inhibitor that inhibits differentiation of T cells into Th1 cells. The inhibitor that inhibits differentiation of T cells into Th1 cells contains, as an active ingredient, pitavastatin or a salt thereof.
EP2118118A2 Mediated cellular delivery of lna oligonucleotides The present invention relates to novel modified oligomeric compounds linked to one or more metal chelators and to methods of making and using such compounds. The invention further relat.es to methods of enhancing the cellular uptake of oligomeric compounds comprising conjugating a metal chelator to those.
CN103550136A Transmucosal delivery devices with enhanced uptake The present invention provides methods for enhancing transmucosal uptake of a medicament, e.g., fentanyl or buprenorphine, to a subject and related devices. The method includes administering to a subject a transmucosal drug delivery device comprising the medicament. Also provided are devices suitable for transmucosal administration of a medicament to a subject and methods of their administration and use. The devices include a medicament disposed in a mucoadhesive polymeric diffusion environment and a barrier environment.
CN101102995A Process for preparing substantially pure tolterodine tartrate The present invention provides substantially pure Tolterodine.
WO2014019344A1 Bridged ring compounds as hepatitis c virus (hcv) inhibitors and pharmaceutical applications thereof Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
CN101002789A Suppository containing slow releasing three-D fungicidin A slowly-released suppository for treating vaginitis, pruritus vulvae, leukorrhea, etc is proportionally prepared from nysfungin, VE, VA, VD2, fatty acid glyceride mixture, and acrylic resin.
WO2009092276A1 Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof The bicycle-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents of formula (I) are the same as the description.
CN102488657A Fullerenol solid lipid nano-particles, preparation method thereof, and application thereof The invention belongs to the field of radiation protection, and specifically relates to nucleus-targeting fullerenol solid lipid nano-particles with a radiation protection function. The fullerenol solid lipid nano-particles comprises: stearic acid, cholesterol, lecithin, corn oil, Tween-80, fullerenol powder, and diethylstilbestrol. According to the invention, stearic acid, cholesterol, lecithin, corn oil, fullerenol powder, and diethylstilbestrol are sufficiently dissolved in ethanol; the mixture is well mixed; ethanol is removed by rotary evaporation; the mixture is slowly dropped into an aqueous solution of Tween-80 with a same temperature; when dropping is finished, the mixture is stirred and well mixed, such that C60(OH)24-SLN-E primary emulsion is obtained; the C60(OH)24-SLN-E primary emulsion is subject to high-pressure homogenizing, and is cooled, such that a required product is obtained. The fullerenol solid lipid nano-particles provided by the invention can penetrate various biological barriers and nuclear membranes, and carry fullerenol into nuclei with high efficiency. Therefore, free radicals in the nuclei can be removed, such that the radiation protection function can be realized.
WO2013049365A3 Selective metabolic approach to increasing oral bioavailability of phenylephrine and other phenolic bioactives Presystemic metabolism in intestine of bioactives such as phenylephrine is avoided by administering a subject (human or animal) the bioactive (e.g., phenylephrine) in combination with one or more inhibitors of sulfation (e.g., sulfotransferase enzymes aka SULTs). This can also be enhanced be co-administering inhibitors of monoamine oxidases aka, MAOs, and uridine diphosphate glucoronysl transferases, aka UGTs. Preferably the inhibitors are GRAS compounds. The one or more inhibitor compounds inhibit the enzymes responsible for rapid presystemic metabolism, thus allowing the bioactives (e.g., phenylephrine) to be more readily absorbed intact into the circulatory system.
US20060014752 Heterocyclic anti-epileptogenic agents and methods of use thereof Methods and compounds, such as β-heterocyclic-β-amino acids, useful for the inhibition of epileptogenesis are disclosed. Methods for preparing and using the β-heterocyclic-β-amino acids of the invention are also described.
CN103316353A Ice laser treatment device carrier liquid and preparation method thereof The invention relates to an ice laser treatment device carrier liquid and a preparation method thereof, wherein the ice laser treatment device carrier liquid comprises, by weight, 0.5-5% of hydroxyethyl cellulose, 0.005-0.015% of methylchloroisothiazolinone, and the balance of deionized water. According to the present invention, hydroxyethyl cellulose is adopted as a film forming agent, and has advantages of simple component, rapid film forming, good water retention performance and high stability compared with the film forming agent formed by carrying out a reaction of more than two different substances in the prior art; and the ice laser treatment device carrier liquid adopting deionized water and hydroxyethyl cellulose as main components is added with methylchloroisothiazolinone and/or 2-methyl-4-isothiazolin-3-one, such that the ice laser treatment device carrier liquid has a sterilization and sterilization function.
US7160911 Diarylcycloalkyl derivatives, process for their preparation and their use as pharmaceuticals Diarylcycloalkyl derivatives, process for their preparation and their use as pharmaceuticals The invention relates to diarylcycloalkyl derivatives and to their physiologically acceptable salts, racemates and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.
WO2006040451A2 Novel 9h-pyrido[2,3-b]indole derivatives serving as cdk and gsk3 inhibitors, method for the preparation thereof, and the pharmaceutical compositions containing such compounds The invention relates to novel 9H-pyrido[2,3-b]indole derivatives of formula (I), to the pharmaceutical compositions containing such compounds, and to the use thereof for manufacturing a medicament used in the treatment or prevention of cancers, Alzheimer's disease, Parkinson's disease, cerebral vascular accidents, amyotrophic lateral sclerosis (ALS), viral infections, autoimmune diseases, and neurodegenerative disorders.
US20090012049 Use of an Unsaponifiable Extract of Plant Pulp in the Treatment of Skin Ageing. The field of the present invention relates to the use of an unsaponifiable extract of plant pulp in the preparation of a cosmetic, pharmaceutical or nutraceutical product intended for treating and/or preventing skin disorders associated with ageing.
US20100260738 Uses and methods relating to ndr kinase expression and/or activity The present invention relates to the diagnosis, prognosis or predisposition of developing cancer, especially lymphoma. The invention also relates to gene therapy and identification of potential new therapeutic agents for treating cancer such as lymphoma.
CN101049299A PravastatinNa pills, and preparation method A dripping pill of pravastatin sodium for treating hyperlipemia is prepared from the pravastatin sodium and the matrix of dripping pill. Its preparing process is also disclosed.
US20100074908 Human synthetic single-chain antibodies directed against the common epitope of mutant P53 and their uses Isolated polypeptides, isolated polynucleotides or expression vectors encoding same, viral display vehicles which can be specifically bind an exposed epitope shared by mutant, but not wild type, p53 protein are provided. Also provided are methods of inducing apoptosis and treating cancer as well as diagnosing a p53-related cancer using the isolated polypeptides uncovered by the present invention.
US20060035979 Inhibitors of transcription factor NF-kappaB The present invention provides pharmaceutical compositions of salicylanilide inhibitors of transcription factor NF-κB, and methods for treating diseases in which activation of NF-κB is implicated. More specifically, the present invention provides methods of treatment of a variety of diseases associated with NF-κB activation including inflammatory disorders; particularly rheumatoid arthritis, inflammatory bowel disease, and asthma; dermatosis, including psoriasis and atopic dermatitis; autoimmune diseases; tissue and organ rejection; Alzheimer's disease; stroke; atherosclerosis; restenosis; cancer, including Hodgkin's disease; certain viral infections, including AIDS; osteoarthritis; osteoporosis; and Ataxia Telangiestasia by administering to a patient in need thereof a compound of the present invention.
EP2510931A1 Therapeutic medium for preventing and treating adenomas and prostatitis The invention pertains to the field of the chemical-pharmaceutical industry, and relates to the production of a therapeutic medium for preventing and treating adenomas and prostatitis and for increasing potency. The therapeutic medium contains the following ingredients: flower pollen, bee brood, ascorbic acid, vitamin E and carriers. This medium can be used by aged persons having an increased arterial pressure.
WO2013027840A1 Hydrous adhesive skin patch The purpose of the present invention is to provide a hydrous adhesive skin patch which contains lidocaine and can be applied in a uniform thickness easily. This hydrous adhesive skin patch comprises a support and an adhesive agent layer arranged on the support, wherein lidocaine or a pharmacologically acceptable salt thereof, a hydrophilic adhesive agent, and diethylene glycol or a diethylene glycol monoalkyl ether are contained in the adhesive agent layer. The diethylene glycol monoalkyl ether is preferably at least one compound selected from the group consisting of diethylene glycol monomethyl ether, diethylene glycol monoethyl ether and diethylene glycol monobutyl ether.
CN102702210A Application of phthalocyanine metal complex containing piperazine ethyoxyl modified groups The invention belongs to the field of the preparation of photodynamic medicines or photosensitizers, and discloses application of a phthalocyanine metal complex containing piperazine ethyoxyl modified groups. The phthalocyanine metal complex can be used for preparing the photodynamic medicines or the photosensitizers, and has the characteristics that the phthalocyanine metal complex is amphipathic, absorption spectrum red is transferred to wavelengths which facilitate the penetration of tissues of human bodies, and the capacity of generating active oxygen by photosensitization is high.
US20050004088 Hormonal contraceptive product The present invention relates to a hormonal contraceptive product having two hormonal components, an estrogen and a gestagen, and a method for the continuous suppression of the menstrual cycle by uninterrupted administration of the product of the invention.
CN101524347A Intraocular implant for preventing and treating after cataract and preparation method thereof The invention relates to intraocular implant for preventing and treating lens posterior capsule opacification (after cataract), a preparation method thereof and application of Docetaxel in preparing medicines for preventing and treating lens posterior capsule opacification. The implant comprises Docetaxel and at least one kind of polymer carrier, wherein the content of Docetaxel in the preparation is 0.01 to 20 percent; and the mixture ratio of the polymer carrier to medicines ranges from 5:1-10,000:1. The preparation method comprises the following steps: evenly mixing the Docetaxel and polymer carrier monomer in proportion; adding activating substance and/or crosslinking agent and introducing nitrogen for protection; carrying out reaction at a temperature of between 50 and 100 DEG C in a die till the product takes shape; and finally, carrying out sterilization. The medicines and the polymer carrier are made into in-capsule implant and the preparation is implanted into the hollow cavity of a lens capsule after extracapsular cataract extraction to play a role in restraining proliferation of lens epithelial cell for a long time.
WO2011014775A1 Modulation of sgk1 expression in th17 cells to modulate th17-mediated immune responses The inventors have made the surprising discovery that SGK1, a serine/threonine kinase previously described as being involved in regulation of cellular sodium homeostasis, has a novel and unexpected function in the differentiation and function of a specific subset of CD4 T cells, the TH17 lineage. Described herein are methods and compositions for modulation of TH17 cell differentiation, proliferation, and/or function that rely upon modulating the activity or expression of SGK1. Such methods and compositions are useful in the treatment of disorders including autoimmune diseases, chronic inflammatory conditions, infectious diseases, and cancer.
CN101524429A Gel film agent for treating eczema, ecthyma, and impetigo The invention relates to a Juisheng san gel film agent for treating eczema, ecthyma, and impetigo, which is characterized in that sodium carboxymethyl cellulose and other gels are compounded into a paste matrix; and the film agent carries carbon powder which is obtained by burning and baking a Juisheng san water suspending agent and residue thereof. The film agent comprises the following advantages that: 1, the film agent has hemostasis function; 2, the film agent has the function of inhibiting the growth of bacteria; 3, the film agent can prolong the time of medicament release; 4, the film agent generates the bioadhension so as to firmly adhere to an afflicted part; 5, the film agent has adsorption function on moisture, ulcer and ichor of the skin; 6, the film agent has the functions of inhibiting the growth of fibrocyte and reducing scars; 7, the film agent does not adhere to the skin and is easy to remove so as to not cause secondary bleeding and damage; 8, the film agent has good ventilation property; 9, the film agent makes a preparation more stable; and 10, the film agent has convenient use.
CA2453687A1 Therapeutic composition containing at least diflomotecan and capecitabin e Disclosed herein is the use of diflomotecan in synergistic combination with capecitabine, for the preparation of a medicament intended to treat cancer. Also disclosed is the product comprising a first component consisting of a therapeutically composition containing diflomotecan as active ingredient, and a second component consisting of a therapeutically composition containing capecitabine as active ingredient, as synergistic combination product for simultaneous or separate use, or use sequenced over time for treating cancer.
CN103432149A Compound capsule containing ilaprazole sodium composition, and preparation method of compound capsule The invention relates to a compound capsule containing an ilaprazole sodium composition, and a preparation method of the compound capsule. The capsule comprises an ilaprazole sodium enteric pellet, a clarithromycin sustained-release pellet and an amoxicillin sustained-release pellet, wherein a prescription mainly contains 5-10mg ilaprazole sodium, 400-600mg clarithromycin and 900-1100mg amoxicillin. The capsule has a remarkable effect on treating a peptic ulcer, and has the advantages that the capsule becomes effective quickly, and is high in effect, convenient to take and low in cost; the bioavailability can be improved; and helicobacter pylori can be killed thoroughly.
WO2014116593A1 Novel traps in the treatment of macular degeneration The present invention is directed to compounds of formula (A): pharmaceutical compositions, and methods of use for treating, reducing a symptom of or reducing the risk of macular degeneration.
WO2013155204A3 Compositions and methods for inhibiting expression of the alas1 gene The invention relates to double- stranded ribonucleic acid (dsRNA) compositions targeting the ALAS1 gene, and methods of using such dsRNA compositions to alter (e.g.,inhibit) expression of ALAS1.
US20120157529 Composition and Method for Prevention, Mitigation or Treatment of an Enteropathogenic Bacterial Infection The present invention embraces the use of palmitoleic acid, or a derivative, mimetic, or extract containing the same, to decrease the expression of bacterial virulence factors thereby preventing, mitigating, or treating bacterial infection.
CN102924622A Helianthus annuus polysaccharide and preparation method thereof The invention relates to extraction of active ingredients and biological activity of the active ingredients from waste sunflower discs generated in sunflower recovery process, and particularly belongs to the fields of preparation of health foods and pharmaceuticals and refuse reclamation. The invention provides a method for extracting polysaccharide from sunflower discs, which mainly comprises the following steps of choosing materials, crushing, soaking, enzymolysis, filtering, concentrating and drying in vacuum. The invention also relates to applications of sunflower polysaccharide in the preparation of health foods and pharmaceuticals, especially the applications in the preparation of health foods and pharmaceuticals with immune enhancing function. The main use of the method provided by the invention is to extract, process and reutilize the active ingredients in waste sunflower discs, so as to achieve the purpose of waste utilization and turning waste into wealth.
US20120149727 Prasugrel in non-crystalline form and pharmaceutical composition thereof The present invention relates to prasugrel or a pharmaceutically compatible salt thereof, compositions that contain this active substance and pharmaceutical compositions that contain this active substance or a composition containing this active substance. The present invention further relates to methods for producing the novel compositions.
EP1608367A1 Pramipexole for reducing excessive food intake by children The invention relates to the use of dopamine receptor agonists for producing a pharmaceutical for reducing excessive food intake.
US20120058160 Particulate materials Embodiments of the invention relate to particles of active substances, methods for preparing the particles, formulations containing the particles, and metered dose inhalers containing such particles or formulations. In one embodiment, a composition of an aerosol formulation is provided and contains a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 10 μm suspended in a hydrofluorocarbon fluid vehicle at a concentration within a range from about 0.2% w/v to about 5% w/v. The aerosol formulation exhibits a flocculation volume of about 85% or greater about 1 minute after mixing the particulate active substance and the hydrofluorocarbon fluid vehicle. The particulate active substance contains an alkaloid ergotamine, pharmaceutically acceptable salts thereof, analogues thereof, or derivatives thereof. In some examples, the alkaloid ergotamine contains dihydroergotamine, such as dihydroergotamine mesylate and the hydrofluorocarbon fluid vehicle contains HFA 134a, HFA 227ea, or mixtures thereof.
CN102872256A Treatment type vagina gel and preparation method thereof The invention provides a treatment type vagina gel and a preparation method thereof. The treatment type gel comprises phellodendron, kuh-seng, fructus forsythiae, fructus cnidii, calcined alum, cuttle-bone, dandelion, radices salviae miltiorrhizae, spina gleditsiae, sargentgloryvine stem, radices paeoniae rubra, herba leonuri, radices lithospermi, oldenlandia diffusa, radix rehmanniae recen, honeysuckle, lignum millettiae, catechu and the like, can improve the immunization capacity of the vagina, meanwhile has functions of sterilization, antiphlogosis and peculiar smell clearing, can achieve auxiliary effects of the treatment of various gynecological diseases, and is less in side effects.
WO2007034924A1 METALLO-β-LACTAMASE INHIBITOR Disclosed is a metallo-β-lactamase inhibitor which can inactivate a β-lactam antibiotic and recover the anti-bacterial activity of the β-lactam antibiotic. A maleic acid derivative having a structure of the general formula (I) has an inhibitory activity against metallo-β-lactamase. The use of the compound (I) in combination with a β-lactam antibiotic enables to recover the anti-bacterial activity of the β-lactam antibiotic against a bacterium capable of producing mettalo-β-lactamase.
WO2008107099A1 Drug comprising at least one gestagen The present invention relates to the use of at least one gestagen selected from the group consisting of chlormadinone acetate, 3α-hydroxy-6-chlor-17α-acetoxy-4,6-pregnadien-20-one (3α-hydroxy-chlormadinone acetate), and 3ß-hydroxy-6-chlor-17α-acetoxy-4,6-pregnadien-20-one(3ß-hydroxy-chlormadinone acetate) of the gestagen components, and optionally at least one estrogen selected from the group consisting of ethinyl estradiol, estron, estriol of the estrogen components, and estradiol for the production of a drug for the treatment and/or for the prevention of melasma, and optionally for simultaneous hormonal contraception, or optionally for simultaneous hormone replacement for women.
CA2434731C Modular infusion device and method A device (10) for delivering fluid including a disposable assembly (800) having an exit port assembly (70) and a metering portion of a dispenser (40) for controlling fluid flow to the exit port assembly (70), and a reusable assembly (700) having a control portion (46) of the dispenser (40) adapted to control the metering portion of the dispenser (40) upon attachment of the reusable assembly (700) and the disposable assembly (800), a local processor (50) connected to the dispenser (40) and programmed to cause fluid flow to the exit port assembly (70) through the dispenser (40) based upon flow instructions, and a local wireless communication element (60) connected to the local processor (50) for receiving flow instructions from a remote wireless device (100). The assemblies (700, 800) are adapted to be removably attached, and a power source (80) is contained in the disposable assembly (800) for providing power to the reusable assembly (700) upon attachment of the reusable assembly (700) and the disposable assembly (800)..
CN101219147A Dectancyl mastication tablet for dogs and cats The invention discloses a dexamethasone acetate chewable tablet for canine and feline, which overcomes the shortcoming of poor palatability of the existing tablet, facilitates that the dexamethasone acetate chewable tablet is chewed and absorbed thoroughly by the cats and dogs to guarantee effective dosage, increases the cure rate of canine and feline diseases and reduces drug waste. The dexamethasone acetate chewable tablet of the invention comprises that (by weight percentage): 1-5 percent of aspartame, 20-30 percent of mixture of oral glucose and skim milk powder (the proportion of the oral glucose and the skim milk powder is 1:1-1:4); 40-60 percent of excipient, 0.5-1 percent of fluidizer and 10-30 percent of dexamethasone acetate respectively.
CN103191140A Anti-tumor activity of emodin-8-O-beta-D-glucoside and new application thereof The invention relates to anti-tumor activity of emodin-8-O-beta-D-glucoside and new application thereof in preparation of tumor treatment and prevention medicaments or food. In a certain concentration range, the emodin-8-O-beta-D-glucoside can selectively kill multiple cancer cells such as human liver cancer cells, colorectal cancer cells and the like, and does not affect the vitalities and functions of human normal cells. Therefore, the emodin-8-O-beta-D-glucoside can be used for preparing anti-tumor medicaments and medicaments or food for preventing tumors.
US7507768 Administering a tablet designed to control moisture containing metformin and glipizide and having a protective coating or finishing layer; glipizide does not hydrolyze and the metformin is compressible; does not have an enteric coating An antidiabetic pharmaceutical formulation is provided, especially adapted for treating Type II diabetes, which includes a combination of metformin and glipizide in a manner to control moisture in the formulation so that the glipizide does not hydrolyze, yet the metformin is compressible, if necessary. A method for treating diabetes is also provided employing the above formulation.
CN103083342A Application of flavan compound in preparing anti-complement medicines The invention belongs to the field of pharmacy, and relates to a novel application of a flavan compound in preparing anti-complement medicines. According to the invention, a modern pharmacological screening method is applied, and researches are carried out upon anti-complement active substances in plant medicines. According to the invention, the flavan compound is obtained by separation from an n-butanol extract of a commelinaceae plant commelina and an n-butanol extract of a polygonum plant fagopyrum. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect upon classical pathway and alternative pathway of a complement system. The CH50 of the inhibition effect of the compound upon the classical pathway of the complement system is 0.13 (plus or minus 0.03)-0.78 (plus or minus 0.06) mM, and the AP50 of the inhibition effect of the compound upon the alternative pathway of the complement system is 0.12 (plus or minus 0.01)-1.00 (plus or minus 0.15) mM. The compound can be used for preparing anti-complement medicines.
WO2010103338A1 Analogues of 1,3-bis(4-nitrophenyl)triazenes, their pharmaceutically acceptable salts and n-acyl derivatives for tumour treatment The present invention refers to analogues of 1,3-bis(4-nitrophenyl)triazenes, their pharmaceutically acceptable salts and N-acyl derivatives for the treatment of different types of tumours. Said compounds show cytotoxicity at very low concentrations (IC50 0,22 to 12,8 μM), and good solubility. These compounds can be used in the treatment of tumour patients as single drugs or in combination with other cytostatics.
CN101077883A Small interference RNA sequence of hepatitis B virus gene and preparation method thereof The present invention provides small interference RNA (siRNA) sequence of hepatitis B virus (HBV) and its preparation process. The sequences of two pairs of HBV ayw subtype S gene DNA template for transcription of siRNA are provided in SEQ ID Nos. 1-4, and specific siRNA for HBV ayw subtype gene is first synthesized through extracorporeal transcription and then transfected to cell for inhibit HBV gene expression. The method of the present invention can obtain great amount of anti-HBV siRNA fast economically and provide the research experiment and clinical application of HBV with great amount of siRNA.
US20120093898 Metal Ion Nanoclusters A composition containing a plurality of water-soluble nanoclusters ranging from 2 nm to 500 nm in diameter. Each of the nanoclusters contains one or more metal cations, one or more anions, and one or more water-soluble ligands. Also disclosed is a method of using the composition for treating various disorders such as anemia, heartburn, and diabetes.
CN102120752A Compound with effects of resisting inflammation and platelet activation and aggregation as well as preparation method and application thereof The invention relates to a compound with effects of resisting inflammation and platelet activation and aggregation as well as a preparation method and application thereof. The compound has the structure of (25R)-26-oxy-beta-D-glucopyranose-5alpha-furostanol-3beta,12beta,22,26-tetraalcohol-3-oxy-beta-D-glucopyranose(1->2)[beta-D-glucopyranose(1->3)]-beta-D-glucopyranose(1->4)-beta-D-galapyranoside. The effects of the compound in the field of cardial vessels are comprehensively researched from platelet aggregation, platelet activation, platelet calcium ion variation, platelet activation signal transduction pathway and expression of platelet activation relevant inflammatory factors in the invention for the first time. Results show that the compound is a substance found to be with a strong effect on resisting platelet aggregation so far in the allium macrostemon saponin compounds, which has the stronger effect than that of aspirin with the same concentration; and the compound simultaneously has an obvious effect on resisting relevant platelet inflammations. The compound provided by the invention can be applied to medicines for treating thrombus and atherosclerosis.
US7592451 Glyceraldehyde 3-phosphate dehydrogenase (GADPH) inhibitors and screening compounds The present invention relates to a compound having the formula where Z is an amine, phenoxy, or thiol-containing group, and Y is an alkyl-containing amine. Methods of producing such compounds and using them to treat patients with diabetes and obesity are also disclosed. The present invention also relates to treating such conditions with GADPH inhibitors and screening compounds useful for treating such conditions by using GADPH inhibitors. Compounds can also be screened for their effectiveness in modulating diabetes and obesity with a C. elegans strain.
WO2010008317A1 Agent for activating stem cells The invention relates to medicine, in particular to medicinal preparations directed at activating their own stem cells. The aim of the invention is to develop a non-toxic agent which does not produce side effects and is used for activating the stem cells of an organism. The method for producing the agent involves taking a 37-40% medicinal formaldehyde solution and adding it into a 0.9-0.95% sterile sodium chloride solution used for injections in such a way that a 0.00003-0.003% formaldehyde solution is obtained. The agent should be stored in a dark place at a temperature of 15-35°C.
CN102973593A Application of dextran sulfate in preparing medicament for treating hepatic fibrosis The invention discloses novel application of dextran sulfate in preparing a medicament for treating hepatic fibrosis. The medicament can be used for inhibiting inflammatory reaction in hepatic fibrosis attaching process, so that attack or symptom worsening of hepatic fibrosis can be inhibited. Dextran sulfate has good curative effect in a carbon tetrachloride induced animal model; and the medicaments used in the application can be easily acquired, low in price and stable in properties, are convenient to store and transport, and have wide application prospect.
WO2012176668A1 Lidocaine-containing cataplasm A lidocaine-containing cataplasm comprising a backing layer and an adhesive agent (plaster) layer laminated on the surface of the backing layer, wherein the adhesive agent (plaster) layer contains at least one component selected from the group consisting of lidocaine and pharmaceutically acceptable salts thereof, the total content of lidocaine and the pharmaceutically acceptable salts thereof is 3-8 mass% relative to the total mass of the adhesive agent (plaster) layer, the adhesive agent (plaster) layer additionally contains oleic acid in an amount of 0.3-1 mass% relative to the total mass of the adhesive agent (plaster) layer, and the adhesive agent (plaster) layer has a pH value of 6.8-7.4.
CN101301466A Medicament for treating AIDS The invention relates to a drug, in particular to a drug for treating AIDS. The drug is characterized in that the drug is a solution containing 1000 to10000mg Mannatide per 1000 ml; the solution is a Mannatide-containing and anti-HIV drug. The drug has no cumulative toxicity in organism and because the drug does not work by refraining protease and reverse transcriptase of virus, but kills HIV directly, no resistance is produced. The drug acts on bone marrow hematopoietic stem cells directly, activates the human immunity system from the source and can improve the immunity functions of the organism entirely and persistently, showing remarkable treatment effect and fighting against the damage of AIDS virus to the human immunity functions radically. In addition, compared with the prior anti-HIV drug, the drug has a positive treatment effect, a low price and has no toxic and side effect.
CA2793536A1 Methods of treatment of hepatocellular carcinoma The present invention provides methods and compositions for treating hepatocellular carcinoma (HCC) by administering a composition comprising nanoparticles that comprise a taxane and an albumin. The invention also provides combination therapy methods of treating HCC comprising administering to an individual an effective amount of a composition comprising nanoparticles that comprise a taxane and an albumin and another agent, such as an agent that inhibits microtubule disassembly.
CN101367716A Carbon shell bacterium polyketone, preparation and uses thereof The invention discloses novel skeleton dalesconols, which has a general formula described at the right; wherein, 1,3,5,7,9,11,13,15,17,18,19,21,23,25,27 and 29 are the numbers of carbon atomic ordinal, R<1> is H or OH, when R<1> is H, dalesconols is dalesconols A; and when R<1> is OH, dalesconols is dalesconols B. The dalesconols has strong competitive inhibition to the mouse spleen cell proliferation caused by Con A, and has no toxicity to the normal mouse spleen cells; thus the dalesconols can be used as the compound with the functions of immunity and inhibition, and also can be applied to the preparation of the relevant novel medicine.
CN101312965A Morpholine type cinnamide compound Compounds of the formula: (I) [wherein R<1>, R<2>, R<3> and R<4> either identical with or different from each other are a hydrogen atom or a C1-C6 alkyl; X1 is an optionally substituted C1-C6 alkylene; Xa is a methoxy group or fluorine atom; Xb is an oxygen atom or methylene group (provided that when Xa is methoxy, Xb is limited to an oxygen atom); and Ar1 is an aryl, pyridinyl, aryloxy or pyridinyloxy, optionally having a substituent, such as a halogen atom], and pharmacologically acceptable salts thereof, and use thereof as pharmaceuticals.
EP1838335A1 Growth factor composition A composition is provided, which is capable of generating hard tissue when introduced in a mammalian subject and comprises a) an ionic complex of i) chitosan and ii) a negatively charged polysaccharide selected from the group consisting of heparin, heparan sulfate and dextran sulfate, and b)a hard tissue generating growth factor, said ionic complex being a carrier for said hard tissue generating growth factor. Also provided are a method of preparation in vitro of a bone graft substitute using the composition, a kit for carrying out the method, as well as use of the composition in the preparation of a medical device for generation of hard tissue in a mammalian subject in need thereof, and a method of generation of hard tissue at a desired site in a mammalian subject in need thereof.
EP1059911B1 Formulations with an anti-viral effect The invention relates to formulations in solid or liquid form, containing isoquercetin as a natural flavonoid. Said isoquercetin is contained as a light protection filter and/or an antiviral substance. The invention relates to both cosmetic and medical formulations.
US20080181960 Solid dispersion of completely amorphous carotenoids; polyvinylpyrrolidone, hydroxypropylcellulose hydroxypropylmethylcellulose solubility-enhancing polymers;spray dried powder increased bulk density; substantially free of lipids and oils Carotenoid compositions of enhanced solubility and bioavailability are described that contain at least one carotenoid with at least one solubility-enhancing polymer. In one embodiment, the carotenoid is a provitamin A carotenoid such as β-carotene. In another embodiment the carotenoid is a non-provitamin A carotenoid such as lycopene or lutein. Described methods to produce the bioenhanced products include dry blending and solvent spray drying. In accordance with certain embodiments of the invention, the method includes the steps of providing a mixture comprising the carotenoid, a solubility-enhancing polymer and a solvent and removing the solvent to produce an amorphous form of the carotenoid. Products made by the invention's compositions and methods include pharmaceuticals, nutraceuticals, cosmetic, and personal care products for man and animal.
WO2008037421A3 Pharmaceutical compositions comprising an s1p modulator The present invention provides various pharmaceutical compositions comprising an S1P receptor modulator, e.g. an S1P receptor agonist. In one aspect, there is provided a pharmaceutical composition having a coating. In other aspects, rapid disintegrating compositions are provided. In a further aspect, a pharmaceutical composition which is free of sugar alcohols is provided. In another aspect, the invention provides a pharmaceutical composition comprising a coating comprising an S1P receptor modulator.
WO2007039144A1 Pyrrolidine derivatives for treating viral infections Anti-viral agents of Formula (Ia): wherein A represents hydroxy; D represents 3-bromo-4-tert-butylphenyl or 5-bromo-4-tert-butyl-2-fluorophenyl; E represents 1,3-thiazol-2-yl or 5-methylisoxazol-3-yl; G represents methoxymethyl; J represents 1,3-thiazol-4-ylmethyl or 1H-pyrazol-1-ylmethyl; and salts, solvates and esters thereof; provided that when A is esterified to form -OR where R is selected from branched chain alkyl, then R is other than tert-butyl, processes for their preparation and their use in HCV treatment are provided.
US20090087413 Self-complementary aav-mediated delivery of interfering rna molecules to treat or prevent ocular disorders The invention provides methods for delivering interfering RNA molecules to an eye of a patient to treat ocular disorders. In particular, the methods of the invention comprise the use of a self-complementary adeno-associated (scAAV) viral vector that can deliver an interfering RNA molecule to an eye of a patient to inhibit expression of a gene that is associated with an ocular disorder.
US7129239 Dietetics; cardiovascular disorders; strokes; antidiabetic agents, sleep disorders, osteoporosis Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. wherein A is an optionally substituted aryl or an optionally substituted heteroaryl; B is an optionally substituted aryl or an optionally substituted heteroaryl; R1 is hydrogen, (C1–C4)alkyl, halo-substituted (C1–C4)alkyl, or (C1–C4)alkoxy; and R4 is as described herein.
US20110015150 Methods of administering compositions including iron Nutritional or dietary supplement compositions that promote and/or maintain dietary iron absorption through administration of iron with an organic acid and optionally similar iron absorption promoters are provided. Also provided are methods of nutritional or dietary supplementation using one or more compositions that promote and/or maintain health through the prevention, stabilization, reversal and/or treatment of disorders associated with iron deficiency.
CN1887872A Tetrahydro isoquinoline derivative and its prepn process and medicine use The present invention relates to medicine chemistry, and is especially one kind oftetahydro isoquinoline derivative and their preparation process, medicine compositions and medicinal use, especially the use as pain relieving kappa-opium receptor excitant. Their general expression has been shown.
US20100136142 Substituted-4-aryl-1,4-dihydro-1,6-naphthyridinamides and use thereof The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
CN103142998A Oral medical ice for preventing and treating dental ulcer and infection after chemotherapy The invention discloses oral medical ice for preventing and treating dental ulcer and infection after chemotherapy. The oral medical ice includes normal saline; each 100ml of normal saline includes 50-100 micrograms of grain-macrophage colony stimulating factor, 30-100mg of calcium folinate and 250-500mg of lidocaine hydrochloride; and the oral medical ice can be acquired after the normal saline including the above components is frozen to ice. The oral medical ice is used for preventing and treating dental ulcer and infection after high-dose methotrexate chemotherapy or 5-fluorouracil chemotherapy; and the oral medical ice without the calcium folinate can also be used for preventing and treating dental ulcer and infection after other chemotherapies. The oral medical ice disclosed by the invention can be used for alleviating pain, contracting the blood vessels of the oral mucosa, reducing exudation and increasing salivary secretion and can be beneficial to the cleaning of the mouth. The oral medical ice can be slowly molten in the mouth; and the lasting time of the oral medical ice is longer than the time for rinsing the mouth by using collutory. The oral medical ice can be used for improving the chemotherapy tolerance of a patient, promoting the restoration of the oral mucosa ulcer surface, shortening the curing time and reducing the pain of the patient and has no side effects, thereby having good application prospect.
CN101440111B Anti-tumor compound and preparation thereof The invention provides an anti-tumor compound and a method for preparing the same. The method for preparing the anti-tumor compound (3'-{4-[3-(3, 5-di-t-butyl-4-methoxyphenyl)-3-keto-1-propenyl] benzoyl} floxuridine (BOBA-3'- floxuridine ester)) adopts a three-step method of selective protection, esterification and deprotection for synthesis. Compared with floxuridine, BOBA-3'- floxuridine ester has the advantages of prolonging half decay time of the floxuridine, improving fat soluble property of the floxuridine, reducing administration frequency and administration dosage as well as probability and degree of causing adverse reactions; and under the action of in vivo esterase, the BOBA-3'- floxuridine ester can be hydrolyzed into BOBA and the floxuridine, so that the double functional anti-tumor drug which can not only resist metabolism but also induce tumor cells to break up.
CN1679914A Medicinal composition of induced glutathione and ebeselen A composite medicine is prepared from the reduced glutathion or its sodium salt and ebselen in mass ratio of 1:0.05-1. Its advantages are high activity of glutathion-peroxidase (GSH-Px), balanced metabolism of the enzyme associated with Se, and high medical effect.
US20110294745 Solutions of lipophilic substances, especially medicinal solutions The present invention relates to a solution containing at least one water-miscible biocompatible solvent and a lipophilic substance dissolved therein, wherein upon contact with aqueous body fluid the dissolved lipophilic substance is precipitated out of the solution in the form of nanoparticles and a nanosuspension is formed.
WO2013067591A1 Topical formulations for pain management The present disclosure relates generally to the field of pain management, including methods and formulations for the topical management of pain, such as localized pain. The present disclosure further teaches combination therapy to topically ameliorate more intense levels of pain.
US20100068219 Peptides that mimic non-human cross-reactive protective epitopes of the group b meningococcal capsular polysaccharide Peptides that mimic the antigenic features of non human-cross-reactive protective epitopes of the MenB CP and nucleic acids encoding the peptide mimetics are disclosed. Antibodies elicited by these peptides do not bind to polysialic acid in host tissue and thus provide a safe and efficacious method for the treatment and/or prevention of Meningitis B.
CN101857618A Series of quinazoline sugar derivatives used as protein tyrosine kinase inhibitor, preparation method and application thereof The invention provides a quinazoline sugar derivative and a preparation method and application thereof, which can solve the problem of low activity of inhibiting tyrosine kinase in the prior art. The prepared quinazoline sugar derivative has high water solubility and high activity of inhibiting human skin cancer cells A431, and can be used for preparing medicaments for preventing or treating tumors. The quinazoline sugar derivative provided by the invention is a kind of compounds which have novel structures and comprise abundant glycosyl group segments at a 6-bit side chain of a quinazoline parent ring, wherein the raw materials adopted in a method for performing glycosylation on quinazoline rings are readily available; the synthesis method is simple; the purification mode is simple and convenient and quick; and the quinazoline sugar derivative has high water solubility, high biological activity, particularly obvious activity of selectively inhibiting an EGFR, and obvious anti-tumor effect, so the kind of compounds has a wide application prospect in medicaments for preventing or curing tumors. The quinazoline sugar derivative comprises the following structural formula.
CN101513414A Application of 1-acetoxyl group-oleanane-28-carboxylic methyl ether-2,12-diene in preparing medicament for treating skin diseases The invention discloses application of 1-acetoxyl group-oleanane-28-carboxylic methyl ether-2,12-diene in preparing a medicament for treating skin diseases, and provides a pharmaceutical composition. The pharmaceutical composition is characterized by comprising the 1-acetoxyl group-oleanane-28-carboxylic methyl ether-2,12-diene (I) which is taken as an active component and one or more medicinal accessories. In the pharmaceutical composition provided by the invention, the medicinal accessories are all administrative accessories which are suitable for the skin or mucosa.
CN101376654A Water-soluble aminoacid ester derivative of silibinin The invention aims to provide the derivatives of the amino-acid ester of silybin represented by a formula I, wherein R is H, or the side chain of L-amino acid such as methyl, isopropyl, isobutyl, 2-methylpropyl, benzyl and the like.
CN102007873A Intensive artificial propagation method for Myxocyprinus asiaticus An intensive artificial propagation method for Myxocyprinus asiaticus comprises the steps of parent fish selection, induced spawning and hatching. Wherein the induced spawning comprises preparing oxytocic in different doses, administering the oxytocic timely, and designing an oviposition-nest and an oviposition pool, and the hatching comprises designing a hatching pool and determining the special hatching condition. The method of the present invention allows the fry of Myxocyprinus asiaticus to be bred in a large number, the original germplasm to be ensured, the incidence of disease to be reduced, and the survival rate of Myxocyprinus asiaticus to be improved.
CN1976705A 1,1,1- trifluoro-4-phenyl-4-methyl-2-(1H-pyrrolo not 2,3-C|pyridin-2-ylmethyl)pentan-2-ol derivatives and related compounds as glucocorticoid ligands for the treatment of inflammatory diseases and dia Compounds of formula (IA), IB), IC), and (ID) wherein R<1>, R<2>, R<3>, R<4>, R<5>, and R<6> are as respectively defined herein for formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
CN101537109B Medicine for treating throat diseases and preparation method thereof The invention relates to a medicine for treating throat diseases and a preparation method thereof. The medicine is mainly made from dried gypsum, fined talc, essence borax, prepared borax, watermelon frost, calomel, pearl powder, menthol, notoginseng essence, 30-100 parts of polyphylla rhizoma paridis essence, hairy deerhorn and musk, wherein, the notoginseng essence is dried notoginseng extract,and the polyphylla rhizoma paridis essence is dried polyphylla rhizoma paridis extract. The preparation method comprises the following steps: proportionally weighing various bulk drugs, sterilizing, mixing and grinding the bulk drugs into fine powder, and sieving with a 150-300 mesh sieve to obtain powder or make into buccal tablets after adding auxiliary materials. The medicine has the efficacies of diminishing inflammation, easing pain, reducing phlegm, relieving swelling and relieving stuffy nose, and has special effects on the throat diseases such as acute pharyngitis, chronic pharyngitis, laryngitis, tonsillitis, angina, throat infection, cynanche, sore throat, hoarse voice, aphonia, itchy throat and cough caused by upper respiratory tract infection, red and white throat moths and the like. The medicine has unique preparation process, low cost, high curative ratio and quick effect, and can quickly relieve discomfort symptoms of burning and aching throat, dysphagia and the like.
CN101406496A Prescription for treating prostatitis and other reproductive system diseases of male The invention relates to a formula for treating prostatitis and other male reproductive system diseases. The invention discloses a main compound extracted from mangosteen: Garcinia Mangostana, wherein alpha-mangostin is taken as a main effective constituent and mixed with various commonly used fillers in the medicine industry to prepare various appropriate preparation formulations including tablets, capsules, powder, and suppository; and the various preparation formulations can be used for preventing and treating male reproductive system inflammations such as prostatitis, orchitis, deferentitis and urethritis by means of oral taking or external application. The content of the alpha-mangostin in the product is between 3 and 99.8 percent; and the prepared product can relieve various inflammations, has the function of relieving pain to certain degree, and can be independently used or mixed with other natural substances for use.
CN102066359A Novel heteroaryl carboxamide derivatives The invention is concerned with novel heteroaryl carboxamide derivatives of Formula (I), wherein (II), m, X, Y, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.
CN1561989A Soybean aglycone soft capsule and its preparing method A soybean aglycone softgel is composed of the liquid medicine prepared from soybean aglycone, cosolvent, diluent, emulsifierand disintegrant and the shell prepared from gelatin, glycerine, opacifier and antiseptic.
US20090082450 Deuterium-enriched diclofenac The present application describes deuterium-enriched diclofenac, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN102861050A Application of Houttuynoid A in medicine for treating pancreatic cancer The invention discloses application of Houttuynoid A in preparing medicine for treating pancreatic cancer, which belongs to the technical field of new application of the medicine. According to the assessment on the antineoplastic activity through in-vitro MTT method, Houttuynoid A has an obvious inhibiting effect on the growth of human pancreatic cancer cell strains PANC-1 and BXPC-3. Therefore, Houttuynoid A can be used for preparing the medicine for preventing pancreatic cancer, and has a favorable development and application prospect. The application of the Houttuynoid A in preparing the medicine for treating pancreatic cancer, which is provided by the invention, is disclosed for the first time, and because the skeleton type belongs to brand-new skeleton type, the inhibiting activity of Houttuynoid A to pancreatic cancer cells is extremely strong.
US20090162283 Diagnostic and remedy for disease caused by amyloid aggregation and/or deposition To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation and/or deposition. The invention provides a compound represented by formula (1): (wherein X1 represents an optionally substituted bicyclic heterocyclic group; X2 represents a hydrogen atom, a halogen atom, or a chelate-forming group; ring A represents a benzene ring or a pyridine ring; and ring B represents an optionally substituted 5-membered aromatic heterocyclic group which is bonded to the benzene ring or the pyridine ring via a carbon atom of ring B), a salt thereof, a solvate of any of these, or a transition metal coordination compound of any of these, and a diagnostic, preventive, or therapeutic drug containing the same.
EP2368988A1 Modulation of Glucocorticoid Receptor Expression Compounds, compositions and methods are provided for modulating the expression of glucocorticoid receptor. The compositions comprise antisense compounds, particularly antisense oligonucleotides which have particular in vivo properties, targeted to nucleic acids encoding glucocorticoid receptor. Methods of using these compounds for modulation of glucocorticoid receptor expression and for treatment of diseases are provided.
US20100278724 Inhibition of migration and induction of cell death by the type ii collagen amino propeptides The present invention provides combinations and methods for inducing cell death, inhibiting angiogenesis, and inhibiting cell migration. In particular, the present invention provides methods for inducing cell death in a cell expressing an αvβ3 and/or an αvβ5 integrin.
CN101392030A Middle substitution degree carboxymethyl pachyman, preparation method thereof and use thereof The invention relates to intermediate substitution degree carboxymethylpachymaran (CMP for short) and a preparation method and the application thereof. With water as a medium, pachynaran and chloroactic acid react with appropriately excessive sodium hydroxide at the temperature of 50 DEG C to 59 DEG C for a period of 8h to 24h. The substitution degree (D.S) of the carboxy methyl of the intermediate substitution degree CMP is in a range of more than 0.5 but less than 1.0 and the molecular weight (MW) thereof is larger than 10<6> Dalton. The preferable application of the intermediate substitution degree CMP is to serve as the bulk drug of CMP frozen dry powder injectors or CMP injection.
EP1228030B1 Benzenoid derivatives of 15-hydroxyeicosatetraenoic acid and methods of their use in treating dry eye disorders Benzenoid HETE derivatives and methods of their use for treating dry eye are disclosed.
US20100173968 Sub-type selective azabicycloalkane derivatives Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide, ketone, and ester compounds prepared from certain azabicycloalkane carboxylic acids. The resulting compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, such as those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).
USRE43029 Process for preparing a creatine heterocyclic acid salt and method of use This invention relates to a process for the synthesis and method of use of an effective amount of a creatine heterocyclic acid salt for the regulation athletic function in humans.
CN102688235A Lercanidipine hydrochloride composite tablet, preparation method thereof and application as antihypertensive drug The invention provides a lercanidipine hydrochloride composite tablet, a preparation method of the tablet and application as antihypertensive drug. The tablet is a gastric floating tablet prepared from active components (lercanidipine hydrochloride and berberine hydrochloride) and adjuvants. The pharmaceutical composition can effectively treat hypertension induced by diabetes, and has certain protective effect on kidney. According to the invention, the above pharmaceutical composition is prepared into the gastric floating tablet, thereby facilitating drug absorption, improving bioavailability, and achieving better curative effect on hypertension.
CN101306074A Anti-alcohol and liver- protection medicine composition The invention provides a medicine combination having the functions of combating intoxication and protecting liver. The combination primarily consists of kudzu root extract, ginkgo leaf extract, L-cysteine and cevitamic acid. The combination comprises the following active ingredients by weight parts: 150 to 300 parts of kudzu root extract, 50 to 200 parts of ginkgo leaf extract, 30 to 200 parts of L-cysteine, and 20 to 300 parts of cevitamic acid. The medicament form of the combination provided by the invention has the excellent function of protecting liver, and excellent combating intoxication effect, and has no toxic and side effect.
US20060148828 Combination comprising a CDK inhibitor and a topoisomerase 1 inhibitor for the treatment of cancer and other proliferative diseases A first aspect of the invention relates to a combination comprising a CDK inhibitor and CPT-11. A second aspect of the invention relates to a pharmaceutical product comprising a CDK inhibitor and CPT-11 as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a CDK inhibitor and CPT-11 to a subject.
US20050208135 Monocompartment osmotic controlled drug delivery system The present invention relates to a monocompartment osmotic controlled drug delivery system comprising a poorly soluble drug and at least one alginic acid derivative.
US20110027339 Porous implants and stents as controlled release drug delivery carriers The common premise of synthetic implants in the restoration of diseased tissues and organs is to use inert and solid materials. Here, a porous titanium implant enables the delivery of microencapsulated bioactive cues. Control-released TGFβ1 promoted the proliferation and migration of human mesenchymal stem cells into porous implants in vitro. Upon 4-wk implantation in the rabbit humerus, control-released TGFβ1 from porous implants significantly increased BIC by 96% and bone ingrowth by 50% over placebos. Control-released 100 ng TGFβ1 induced equivalent BIC and bone ingrowth to adsorbed 1 μg TGFβ1, suggesting that controlled release is effective at 10-fold less drug dose than adsorption. Histomorphometry, SEM and μT showed that control-released TGFβ1 enhanced bone ingrowth in the implant's pores and surface. These findings suggest that solid prostheses can be transformed into porous implants to serve as drug delivery carriers, from which control-released bioactive cues augment host tissue integration.
CN101627972B Entecavir orally disintegrating tablet and method for preparing same The invention relates to an Entecavir orally disintegrating tablet for treating hepatitis and a method for preparing the same, which belong to the technical field of medicament. The Entecavir orally disintegrating tablet comprises the following components in percentage by weight: 0.25 to 1 percent of Entecavir, 80 to 90 percent of atomizing dried mannitol, 1 to 4 percent of cross-linked sodium carboxymethyl cellulose or cross-linked polyvidone, 2 to 6 percent of carboxyrnethyl starch sodium, 0.5 to 2 percent of superfine silica gel powder, 0.5 to 2 percent of magnesium stearate, 0 to 2 percent of sweetening agent and 0 to 2 percent of flavoring agent; raw materials are mixed uniformly; and the tabletting operation of fine powder is carried out directly or the rolling pelletization of the fine powder is carried out to carry out the tabletting. The Entecavir orally disintegrating tablet has enough hardness, can meet requirements of production, packaging, storage and transportation, and simultaneously has excellent mouthfeel and shorter disintegrating time.
CN101580552A Preparation method of urtica angustifolia polysaccharide and application thereof The invention relates to a preparation method of urtica angustifolia polysaccharide and an application thereof, belonging to the fields of food and medicine. The method comprises the following steps of: 1, taking urtica angustifolia, drying the urtica angustifolia in the shade, pulverizing the urtica angustifolia, adding water of 8 to 10 times in quantity, heating the mixture to 100 DEG C, and leaching the mixture for 2 to 3 times lasting for 2 to 3 hours every time; 2, filtering the mixture, merging filter liquor, carrying out depressurization concentration and concentrating the mixture to one twelve of the volume of the original liquor; 3, carrying out centrifugation for 15 minutes by 3500 rev/min, taking supernatant fluid and carrying out alcohol precipitation on 95% of ethanol; and 4, carrying out deproteinization for 3 times by a Sevage method, carrying out centrifugation for 10 minutes by 3500 rev/min, concentrating the mixture to volatilize a solvent and carrying out freeze drying. The invention also relates to the application of the urtica angustifolia polysaccharide in the preparation of medicine with an anti-fatigue function. The medicine has obvious anti-fatigue effect, safety and no toxicity.
US20090163499 Imidazole-substituted arylamides as P2X3 and P2X2/3 antagonists Compounds of the formula I: wherein R1 is optionally substituted imidazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
US20110251179 3,4-DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
CN102058573A Application of curcuma wenyujin diterpene compound C in drugs for treating gastrointestinal inflammation The invention discloses application of a curcuma wenyujin diterpene compound C of formula (I) in the drugs for treating gastrointestinal inflammation. The gastrointestinal inflammation comprises one of stomachache, chronic gastritis, acute gastritis, chronic enteritis, acute enteritis and gastric ulcer; and the daily effective dose of the curcuma wenyujin compound C for the human body is 0.001-0.01g/kg. The invention provides a list which can be used for preparing new drugs for treating gastrointestinal inflammation, broadens the drug selection range of the patients and provides new varieties for the screening of the drugs for treating gastrointestinal inflammation; and the curcuma wenyujin diterpene compound C of the invention can play a role of suppressing the inflammation through suppressing the nucleus translocation of NF-kappaB and the expression and secretion of COX-2, TNF-alpha, 1L-1beta and 1L-6 in gastrointestinal cells.
WO2005111002A3 Substituted cycloalkyl derivatives for use in the treatment of respiratory diseases The invention relates to the compounds of formula (1), wherein the groups R1, R2, R3, R4, R5, R6, R7, R8, n, m and X are defined as in the claims and in the description. The invention also relates to the use of these compounds as drugs, especially as drugs for use in the treatment of inflammatory and obstructive respiratory diseases.
CN1863801A Imidazopyridine substituted tropane derivatives with ccr5 receptor antagonist activity for the treatment of HIV and inflammation The present invention provides compounds of formula (I) wherein R<1> and R<2> are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory
US20110046532 composition including a silicone-based polymer and a method of treating skin disorders using the composition A composition is formed by the step of feeding a molecule that has an active oxygen-forming species into a silicone based polymer. The silicone-based polymer is substantially free of pendant groups that are reactive with active oxygen species. Silicone-based polymers have proven scar-healing properties. As such, the composition is useful for treating skin disorders, especially scars, to reduce the appearance of the scars. Furthermore, bacteria and infections may contribute to the formation of scars. The active oxygen-forming species form active oxygen species, which oxidize pathogens including bacteria, viruses, and fungus to sterilize an area in contact with the composition. As a result, the appearance of scars treated with the composition may be even further reduced due to the presence of the molecule having the active oxygen-forming species.
EP2517713A2 A method of treating allergic asthma, allergic rhinitis and atopic dermatitis The present invention relates to a method of treating allergic asthma, allergic rhinitis and atopic dermatitis, more particularly the present invention relates to the use of WF10 for such treatment.
US20070021474 Heterocyclically Substituted Benzoylureas, Process For Their Preparation and Their Use as Pharmaceuticals Heterocyclically substituted benzoylureas, process for their preparation and their use as pharmaceuticals The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the formula I where the radicals are defined as specified, and also their pharmaceutically acceptable salts and processes for their preparation. The compounds are suitable, for example, for treating type 2 diabetes.
US20090186064 Antimicrobial material and method for making the same This invention provides a modified catheter biomaterial that provides both immediate, and long-term microbiocidal effects on otherwise antibiotic-resistant strains of microorganisms. The material, which exhibits good mechanical performance characteristics for medical devices, is composed of a hydrophobic polyurethane (PU), a hydrophilic polyethylene vinyl acetate (PEVA), a soluble silver salt and a sparsely-soluble silver salt. The hydrophobic polyurethane provides the good physical properties, the PEVA the hydrophilicity necessary to allow some water ingress into the catheter, the soluble silver salt for an immediate burst effect, and the sparsely-soluble silver salt for sustained-release over many months postimplantation.
WO2014122670A1 Carbodithioates with spermicidal activity and process for preparation thereof The present invention relates to the synthesis and biological evaluation of compound of formula I as spermicidal agents, and its pharmaceutically acceptable acid salt thereof. The invention provides bis(4- substituted-1-piperazinylthiocarbonyl) disulfide (when n = 0) and alkane-1,n-diylbis(4-substituted piperazine-1-carbodithioate) (when n = 0, 1, 2 or 3) as shown in figure 1 of the accompanying drawing. These compounds are found to be useful for spermicidal activity.
US20090298928 Composition and method for scalp and hair treatment Provided is a composition for scalp and hair treatment, comprising a menthol derivative and a prostaglandin compound having two hetero atoms at the 15 position. The composition of the present invention is effective not only for preventing dandruff and itchy scalp but also for preventing or treating hair loss, baldness, or hair thinness.
US20110052603 method of treatment and agents useful for same The present invention relates generally to a method of modulating tumor necrosis factor-mediated apoptosis and to agents useful for same. More particularly, the present invention contemplates a method of modulating tumor necrosis factor-mediated hepatocyte apoptosis by modulating an intracellular Bim and/or Bid-dependent signalling mechanism. The method of the present invention is useful, inter alia, in the treatment and/or prophylaxis of conditions characterized by aberrant, unwanted or otherwise inappropriate tumor necrosis factor-mediated apoptosis. The present invention is further directed to methods for identifying and/or designing agents capable of modulating the subject Bim and/or Bid-dependent signalling mechanism.
WO2013120980A1 Tricyclic compounds and methods of use therefor The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
US20080064715 I kappa B kinase inhibition; diabetes; (7-Chloro-1H-pyrrolo[2,3-c]pyridin-2-yl)methanol; N-Benzyl-7-chloro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide A compound represented by the formula wherein R1, R2, R3 and R6 are the same or different and each is a hydrogen atom or a substituent; one of R4 and R5 is a hydrogen atom and the other is a group represented by the formula: —C(═X)—R7 wherein X is N—O—R8 or N—NH—R9 wherein R8 and R9 are the same or different and each is a hydrogen atom or a group bonded via a carbon atom; and R7 is a hydrogen atom or a substituent, and the like and a salt thereof have a superior IκB kinase inhibitory activity, and useful as pharmaceutical agents such as agents for preventing or treating diabetes and the like.
CN102133172B Paclitaxel nano micelle and application thereof The invention discloses paclitaxel nano micelle and an application thereof. The paclitaxel nano micelle is prepared from the following components shown in the following (1), (2) or (3): (1) a carrier and paclitaxel, wherein the carrier is a mixture of polyethylene glycol-distearoyl phosphatidyl ethanolamine (PEG-DSPE), D-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS) and dequalinium chloride; (2) a carrier and the paclitaxel, wherein the carrier is a mixture of the PEG-DSPE and the TPGS; and (3) a carrier and the paclitaxel, wherein the carrier is the PEG-DSPE. After the functionalized paclitaxel nano micelle disclosed by the invention is orally taken, the paclitaxel can penetrate through a barrier of gastrointestinal tract, thus the multi-drug resistance (MDR) of drug-resistant breast cancer is overcome. The oral formulation of the functionalized paclitaxel nano micelle disclosed by the invention can avoid the anaphylactic response, can be applied to numerous cancer patients and is also suitable for MDR tumors at the same time, thereby having great advantage compared with the traditional intravenous injection formulation.
EP2123262A1 Polyelectrolyte-encapsulated gold nanoparticles capable of crossing blood-brain barrier A gold-creatine nanoparticle is described, preferably covered with albumin or chitosan, together with a process for its preparation and its use as medicament, in particular for the treatment of stroke. Said gold nanoparticle is capable of crossing the blood-brain barrier.
US20100104570 Semaphorin 7A Plays a Critical Role in TGF-Beta1-Induced Pulmonary Fibrosis and Alveolar Destruction The present invention provides methods of treating a subject diagnosed with, or at risk for developing, pathogenic fibrosis, particularly pulmonary fibrosis. The method of the invention comprises administering to the subject a compound or composition which inhibits semaphorin (SEMA) 7A, SEMA 7A receptors, or downstream effectors. A SEMA 7A inhibitor comprises an antibody, a soluble SEMA 7A receptor, an siRNA, a ribozyme, an antisense, an aptamer, a peptidomimetic, a small molecule, a soluble receptor, or any combinations thereof.
CN103191128A Pharmaceutical composition for preventing regurgitation and aspiration of full-stomach patient at general anesthesia induction stage The invention discloses a pharmaceutical composition for preventing regurgitation and aspiration of a full-stomach patient at a general anesthesia induction stage, and belongs to the technical field of medicines. The traditional general anesthesia induction drug and method aiming at the full-stomach patient cannot effectively prevent regurgitation and aspiration, and endanger life of the patient in a serious situation at present. The technical scheme disclosed by the invention is that lidocaine hydrochloride, midazolam, propofol and remifentanil are mixed according to the ratio to form the pharmaceutical composition. The general anesthesia induction on the full-stomach patient is carried out by the pharmaceutical composition. Thus, regurgitation and aspiration can be effectively prevented; the security of anesthesia is greatly improved; and the pharmaceutical composition is simple and feasible.
CN102228432A Ofloxacin nanoemulsion antibacterial medicine and preparation method thereof The invention belongs to the technical field of antibacterial veterinary medicines, and particularly relates to an ofloxacin nanoemulsion antibacterial medicine and a preparation method thereof. The particle size of the ofloxacin nanoemulsion antibacterial medicine is 1 to 100nm. The ofloxacin nanoemulsion antibacterial medicine consists of the following components in percentage by mass: 0.1 to 7.0 percent of ofloxacin, 20.0 to 35.0 percent of surfactant, 0 to 22.0 percent of cosurfactant, 1.5 to 12.0 percent of oil, and the balance of distilled water. The ofloxacin nanoemulsion antibacterial medicine is light yellow clarified transparent liquid; crystals are not precipitated when the ofloxacin nanoemulsion antibacterial medicine is placed for a long time at the low temperature of -4 DEG C; and the ofloxacin nanoemulsion antibacterial medicine is also not turbid at the high temperature of 60 DEG C, and has a stable pharmaceutical formulation.
WO2010012567A1 Glucocorticoids attached to nitrate esters via an aromatic linker in position 21 and their use in ophthalmology The invention relates to nitrooxy derivatives of fluocinolone acetonide, triamcinolone acetonide, betamethasone and beclomethasone, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other diseases of retina and macula lutea.
CN101787051A Water-soluble carboxyl-bridge dicaryon Pt (II) anti-tumor complex The invention discloses a water-soluble carboxyl-bridge dicaryon Pt (II) anti-tumor complex, which has a chemical name of cis-tetrammine-miu-di (3-acetoxy-1, 1-cyclobutane dicarboxylate-O1, O2) dicaryon platinum (II), and can be synthesized by adopting the method preparing the conventional platinum based anti-cancer drug. The anticancer activity of the complex of the invention is higher than the platinum based drug of carboplatin commonly used in clinic, the toxic side effect of the invention is significantly lower than the toxic side effect of carboplatin, and the invention can be made into lyophilized powder or injecta to be used in the clinical cancer treatment.
WO2007055105A1 Novel anthocyanin compound and method for producing same Disclosed is a novel anthocyanin compound. Specifically disclosed is an anthocyanin compound represented by the following chemical formula [1].
CN1736383A Compound lycopene formulation for women and preparation process thererof Disclosed is a compound tomatine preparation for female and its preparing process, wherein the preparation comprises tomatine, soybean isoflavones, vitamin E, anti-oxidant, capsule stabilizing agent and balancing deflocculating agent. The preparation can be made into the dosage forms of soft capsules, tablets or oral liquids.
US20120052053 Compositions and methods for the treatment of altered alpha-synuclein function Compositions and methods are provided for treating a disorder characterized by α-synuclein dysfunction and/or altered lipid metabolism.
CN102552134A Fat emulsion containing vitamin K1 The invention relates to a fat emulsion containing vitamin K1, and specifically relates to an emulsion composition comprising 0.5-2% of vitamin K1, 7.5-15% of soybean oil, 0.8-2% of phosphatide, 1.5-3% of glycerin, and balance of water. The invention also relates to a preparation method of the emulsion. The emulsion provided by the invention can be used medicinally.
WO2007049119A1 A novel compound, useful for pancreatic lipase inhibition and the process for isolation thereof The present invention relates to a novel, Nonadeca-6-enoic acid-3-(hexadecyloxy-hydroxy-thiophosphoryloxy)-quinoxalin-2-yl ester designated as streptolipin, useful for pancreatic lipase inhibition, isolated from the culture of Streptomyces vayuensis strain N2 having molecular formula (1) and a process for the preparation thereof.
WO2013180403A1 Process for preparing gefitinib and an intermediate used for preparing thereof This invention relates to a method of preparing gefitinib and an intermediate used therein. In the method of preparing gefitinib, the production of an N-alkylated impurity can be suppressed via a simple process, and thus, gefitinib having high purity can be obtained with high efficiency without a complicated separation process such as chromatography, thereby enabling the effective mass production of gefitinib.
US20110275689 Preparation of 3-Pyrrole Substituted 2-Indolinone Derivatives The present invention relates to novel intermediates and further to the use of said intermediates in processes for the preparation of indolinone derivatives, in particular 3-pyrrole substituted 2-indolinones having amide moieties on the pyrrole ring. Such compounds are useful in die treatment of abnormal cell growth, such as cancer, in mammals.
EP1930003A1 Pharmaceutical form containing methocarbamol, meloxicam and betamethasone The present invention relates generally to the pharmaceutical industry, and particularly to the pharmaceutical industry dedicated to the preparation of medicaments for the treatment of exacerbations and acute cases of patients suffering from rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, pain and inflammation relief from acute gouty arthritis, acute and subacute bursitis, tendonitis, synovitis.
CN101371828B Hypocrellin liposome preparation and preparation method thereof The invention discloses a hypocrellin liposome preparation and a preparation method thereof. The hypocrellin liposome preparation comprises the following components according to parts by weight: 1-5 parts of hypocrellin, 40-200 parts of phospholipids, 2.4-12 parts of cholesterol and 50-100 parts of protective agent for freeze drying. The hypocrellin liposome preparation prepared by the high pressure homogenization is characterized in that: the preparation contains no surfactant of Tween; the drug content of the preparation can be increased to more than 1.2 percent from 0.6 percent; the drug concentration of redissolution reaches 1mg/ml, an increase of 100 percent. The invention substitutes the high pressure homogenization for the ultrasonic method so that the quality of the hypocrellin liposome preparation can be assured and the yield greatly increased which meets dual requirements of the industrial production and clinical application of drugs of hypocrellin liposome; meanwhile, the invention substitutes rapid pre-freezing for steady pre-freezing, which can ensure that solid powder of hypocrellin liposome with good monodispersity and more stable morphology after the redissolution is obtained.
CN1813728A Enteric controlled release film coated omeprazol zinc oral solid formulation, oral semi-solid formulation and its preparing method The present invention relates to several kinds of omeprazole zinc oral solid preparation and oral semisolid preparation which are coated with enteric film and their preparation method. These preparations are made up by using omeprazole zinc as main medicine and adding proper quantity of auxiliary material through a certain preparation process. On the basis of said invention said invention also provides a medicine preparation containing omeprazole zinc, poloxamer and/or bianze and its preparation method.
CN101897954A Composition, preparation method thereof and use thereof The invention discloses a composition, a preparation method thereof and use thereof. The composition consists of interleukin 2 and dexamethasone or salts thereof, wherein the content ratio of the interleukin 2 to the dexamethasone or the salts thereof is 200 to 500 thousand international units of interleukin 2: 0.05 to 0.3mg of dexamethasone or the salts thereof. The invention discloses the composition which can be used for preventing and curing allergic diseases and graft versus host diseases and can be further used to cure autoimmune diseases.
WO2009033561A1 Substituted 6-phenylnicotinic acids and the use thereof The present invention relates to novel substituted 6-phenylnicotinic acid derivatives, to methods for the production thereof, to the use thereof for the treatment and/or the prophylaxis of disease, and to the use thereof for producing drugs for the treatment and/or the prophylaxis of cardiovascular disorders, particularly dyslipidemia, arterial sclerosis, and cardiac insufficiency.
WO2006104397A1 Copper antagonist compositions Pharmaceutical compositions having a pharmaceutically acceptable copper antagonist(s) or a pharmaceutically acceptable salts or prodrugs thereof, including copper (II) antagonists, and a pharmaceutically acceptable anti-obesity agent or a pharmaceutically acceptable salt or prodrug thereof, articles and kits and delivery devices containing compositions, tablets and capsules and formulations containing such compositions, and methods of use for treatment of subjects, including humans, who have or are at risk for various diseases, disorders, and conditions.
CN101100470A Tetranuclear bipyrane coumarin compound A tetracyclic-dipyran coumarin compound in the general formula has excellent anti-HIV-Iactivity.
US20090258839 Compositions comprising chitosan suitable for comprehensive therapeutic treatment or comprehensive prevention of the metabolic syndrome The present invention relates to compositions comprising chitosan, in the form of drugs or food supplements, suitable for comprehensive therapeutic treatment or comprehensive prevention of the metabolic syndrome. Also described is their preparation. More generally, the invention concerns the use of chitosan for comprehensive therapeutic treatment or comprehensive prevention of the metabolic syndrome.
EP2296668A1 Compositions for the treatment of hair loss A composition for the treatment or prevention of a disorder resulting in hair loss comprises a cardiac glycoside as active principal.
US20080242666 e.g. (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-6-(1-ethylpropyl)-1-[2(hydroxymethyl)benzyl]-piperazine-2,5-dione; preparation by cyclization The present invention relates to Compound S of Formula (I).
CA2561436A1 Medicinal composition comprising 3-alkoxy-6-allythiopyridazines for prevention or treatment of cancer of the pancreas The present invention relates to a medicinal composition for preventing or treating pancreatic cancer, comprising 3-alkoxy-6-allylthiopyridazine or a pharmaceutically acceptable salt thereof as an effective ingredient. An MTT assay, to assess the viability of cells, and flow cytometric analysis, to measure apoptotic cell death, were performed, and the results, which revealed that the compound and pharmaceutically acceptable salts thereof have preventive and therapeutic activity against pancreatic cancer, are presented herein.
CN101524459A Oil-in-water type garlicin-garlic oil sub-microemulsion as well as method for preparing same The invention relates to an oil-in-water type garlicin-garlic oil sub-microemulsion distributed in an inner phase (oil phase) as well as a method for preparing the same. The formulation of the emulsion contains 0.5 to 3 weight portions of garlicin or garlic oil as a medicament, and the garlicin or the garlic oil is added with a pharmaceutic adjuvant and is prepared into a garlicin sub-microemulsion or a garlic oil sub-microemulsion, wherein the pharmaceutic adjuvant comprises 5 to 20 weight portions of injection oil, 0.2 to 5 weight portions of emulsifier, 0 to 5 weight portions of coemulsifier, 0.5 to 3 weight portions of isoosmotic adjusting agent, a proper amount of antioxidant, a proper amount of pH regulator and a proper amount of injection water. The invention discusses the medicament distribution in oil, an oil/water interfacial film and water when the garlicin or the garlic oil is in an oil-in-water type dispersion system macroscopically and microscopically; more than 98 percent of the medicaments are enwrapped in the oil phase and the medicament free in the water phase is less than 1 percent; and the problem of a garlicin or garlic oil intravenous injection preparation for a hydrophobic dug is solved, the stability of an emulsion thereof is improved, and the vascular stimulation in an intravenous injection is reduced, thus the adaptability of a patient is greatly improved. The oil-in-water type garlicin-garlic oil sub-microemulsion can be applied to the adjuvant therapy of bacteria resistance, cardiovascular and cerebrovascular diseases and tumors.
EP1200607B1 Tet repressor-based transcriptional regulatory proteins The present invention provides a panel of transcriptional activator fusion proteins which comprises both tetracycline controlled transactivator proteins and reverse tetracycline transactivator proteins. These transactivators have novel phenotypes such as alterred basal transcriptional activity in the absence of doxycycline, altered induced transcriptional activity in the presence of doxycycline, or differential induction by tetracycline and analogs of tetracycline.
EP1771453A1 Hepatitis c inhibitor dipeptide analogs The present invention relates to compounds of formula (I): wherein R1, R2, R4, n and m are as defined herein and R3 is selected from: (i) -C(O)OR31 wherein R31 is (C1-6)alkyl or aryl, wherein the (C1-6)alkyl is optionally substituted with one to three halogen substituents; (ii) -C(O)NR32R33, wherein R32 and R33 are each independently selected form H, (C1-6)alkyl, and Het; (iii) -SOvR34, wherein v is 1 or 2 and R34 is selected from: (C1-6)alkyl, aryl, Het, and NR32R33 wherein R32 and R33 are as defined above; and (iv) -CO(O)-R35, wherein R35 is selected from (C1-8)alkyl, (C3-7)cycloalkyl-(C1-4)alkyl, aryl, aryl-(C1-6)alkyl, Het and Het-(C1-6)alkyl, each of which are optionally substituted with one or more substituents each independently selected from halo, (C1-6)alkyl, (C3-7)cycloalkyl, aryl, Het, hydroxyl, -O-(C1-6)alkyl, -S-(C1-6)alkyl, -SO-(C1-6)alkyl, -SO2-(C1-6)alkyl, -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl, wherein the aryl portion of the -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl are each optionally substituted with one to five halo substituents. The present invention further relates to pharmaceutical compositions containing the compounds of formula (I) and methods for using these analogs in the treatment of HCV infection.
CN102091032A o/w type matrine percutaneous absorption microemulsion The invention provides a matrine percutaneous administration new dosage form, namely an o/w type matrine percutaneous absorption microemulsion, and a preparation method thereof. The o/w type matrine percutaneous absorption microemulsion comprises matrine, a surfactant, a cosurfactant, an oil phase and water, and is characterized in that the particle diameter range of the matrine microemulsion is 20-70 cm, and the mean particle size is 31.2 nm. The formula of the o/w type matrine percutaneous absorption microemulsion comprises the following components in percentage by weight: 7% of matrine, 23% of the surfactant, 15% of the cosurfactant, 4.5% of the oil phase, and 0.5% of the water. The o/w type matrine percutaneous absorption microemulsion provided by the invention has the advantage of overcoming the defects of the available matrine injection and matrine oral preparation, such as rapid in vivo release, instable blood concentration and low bioavailability; and the microemulsion permeates skin to enter blood with zero-order kinetics, and has improved bioavailability compared with the oral preparation, so as to provide convenience for infants and chronic disease patients needing long-term administration. The microemulsion also has a distinct effect on inhibiting hypertrophic scar of rabbit ears, and is hopeful to become a candidate medicament for treating hypertrophic scar.
CN101411802A Black plaster for treating hyperosteogeny and preparation method thereof The invention discloses a black plaster for treating hyperosteogeny and a preparation method thereof. The black plaster mainly treats various hyperosteogeny, osteoarthritis, sclerotin regression, periosteum injury and rheumatoid arthritis; raw material medicines are matched with sesame oil and massicot and are decocted to prepare the plaster; and the plaster comprises the following main raw materials in weight portion: 10 portions of angelica, 15 portions of roasted radix paeoniae alba, 6 portions of rhizoma ligustici wallichi, 5 portions of Liao asarum, 6 portions of safflower, 15 portions of radix dipsaci, 10 portions of cortex eucommiae, 20 portions of rhizoma drynariae, 10 portions of achyranthes, 30 portions of lignum millettiae, 6 portions of eupolyphaga, 15 portions of herba lycopodli, 10 portions of tuberculate speranskia herb, 10 portions of roasted mastic, 3 portions of roasted myrrh, 10 portions of radix rehmanniae, 10 portions of rehmanniae vaporata, 15 portions of rhizoma cibotii, 6 portions of herba pyrolae, 15 portions of herba epimedii, 6 portions of radix clematidis, 15 portions of pawpaw, 6 portions of dogwood, 15 portions of mistletoe, 3 portions of deerhorn gelatin, 10 portions of notopterygium incisium, 6 portions of radix angelicae tuhuo, 10 portions of roasted pangolin, 6 portions of ixeritis, 10 portions of parsnip, 6 portions of cinnamon, 15 portions of dioscoreae hypoglaucae, 6 portions of giant knotweed, 10 portions of silkworm larva and the like.
WO2006077412A1 Thienopyrroles useful in the treatment of inflammation There is provided compounds of formula I: wherein the dotted lines, U5 V5 X1, Y, R1, R2 and R4 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.
US8193351 HSP90 inhibitor Compounds represented by formula (1) shown below, pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising such compounds are provided.
US20110218220 Rationally improved isoniazid and ethionamide derivatives and activity through selective isotopic substitution The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including Mycobacterium tuberculosis.
CN1931182A Health food for preventing and treating cardiac and cerebral vascular diseases and its production process The present invention discloses health food for preventing and treating cardiac and cerebral vascular diseases and its production process. The health food is prepared through freezing flavone and biobalide in certain weight proportion at -27 to -40 deg.c; mixing aweto polysaccharide, glossy ganoderma polysaccharide in certain weight proportion and the frozen flavone and biobalide; freeze drying the mixture, and superfine crushing at -5 to 10 deg.c. The health food can lower cholesterol content in blood, preventing cardiac and cerebral vascular diseases, promote blood circulation and raise immunity, and has no any toxic side effect.
US20060031946 Gene therapy with chimeric oligonucleotides delivered by a method comprising a step of iontophoresis The present invention provides a method for enhancing the in vivo delivery of chimeric oligonucleotides, containing for example DNA/2′OMeRNA, into cells of a plant, an animal or a human, comprising a step of applying topically to or injecting into a tissue, or tissue adjacent to a tissue, containing said cells, a composition comprising said chimeric oligonucleotide, followed by, preceded by, or simultaneously to a step of transferring said chimeric oligonucleotide into said cells by iontophoresis, and relates to a gene therapy method comprising the iontophorically transfer of a chimeric oligonucleotide DNA/2′OMeRNA. The present invention is also directed to particular chimeric oligonucleotides DNA/2′OMeRNA capable of inducing or inhibiting the expression of a specific gene involved in eye function by inducing or reverting a mutation in that specific gene, and their use as therapeutic composition for preventing or treating ocular diseases.
US20100261707 Thiadiazole derivatives for the treatment of neurodegenerative diseases This invention provides specifically substituted 1,2,4-thiadiazole derivatives for use in the treatment of an α-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides various methods for producing such substituted 1,2,4-thiadiazole derivatives.
US20050008630 Preservation; nutrients; foods; using ascorbic and citric acid; oxidation resistance; by-product inhibition The present invention provides a stabilization method, a preservation method and the like method of reduced coenzyme Q10, which is useful as functional nutritive foods, specific health foods and the like. Furthermore, the present invention provides a method for efficiently obtaining reduced coenzyme Q10 of high quality and by a method suitable for a commercial production. It is possible to handle and stably preserve reduced coenzyme Q10 under a condition that oxidation by a molecular oxygen is inhibited by contacting reduced coenzyme Q10 with an ascorbic acid and citric acid or a related compound thereof, and thus a stabilized composition is obtained. Moreover, reduced coenzyme Q10 is converted into a crystalline state in such a condition that the formation of oxidized coenzyme Q10 as a byproduct is minimized by crystallizing reduced coenzyme Q10 in the presence of ascorbic acid or a related compound thereof, etc., and thus a reduced coenzyme Q10 crystal of high quality is produced. Furthermore, by successively crystallizing the generated reduced coenzyme Q10 in the presence of ascorbic acid or a related compound thereof after reducing oxidized coenzyme Q10 to reduced coenzyme Q10 using ascorbic acid or a related compound thereof, operations are simplified and minimized, and thus reduced coenzyme Q10 of high quality is produced.
CN102335136A Meropenem medicinal composition for injection and preparation method thereof The invention provides a meropenem medicinal composition for injection and a preparation method thereof. The medicinal composition consists of meropenem and disodium hydrogen phosphate, wherein 1000 pieces of the medicinal composition are prepared from 500 to 1,000g of the meropenem, and 250 to 500g of disodium hydrogen phosphate. The preparation method of the medicinal composition comprises the following steps: rechecking whether the meropenem and disodium hydrogen phosphate are in accordance with the requirements of asepsis and granularity for later use; performing asepsis treatment on an antibiotic bottle and an operation vessel, standing after the moisture of the antibiotic bottle is qualified; mixing; filling; plugging; screwing a cover; testing by use of a lamp; and packaging and sending into a warehouse. The meropenem medicinal composition has simple prescription and excellent stability, and is suitable for long-term storage and industrial large-scale production.
US7354570 Extract of Sanguis Draxonis, Radix Paeoniae Rubra, Indigo Naturalis, 1-Halloysitum Rubrum, Catechu, Calcined Alumen, Rhizoma Bletillae and Calamina; enema This invention provides a preparation of traditional Chinese medicinal materials for the treatment of ulcerative colitis and the processed method thereof. The preparation of present invention is prepared from Sanguis Draxonis, etc. The processed method of the preparation comprises the steps of (a) decocting Radix Paeoniae Rubra, Catechu and Calcined Alumen with water; (b) mixing Indigo Naturalis and Sanguis Draxonis thoroughly, with PEG solution added; (c) mixing the sifted Rhizoma Bletillae, the above-mentioned aqueous decoction and the Indigo Naturalis and Sanguis Draxonis in PEG solution thoroughly, followed by adding Halloysitum Rubrum and Calamina thereto and grinding together, finally the enema is prepared after water being added. The enema of present invention is highly effective in the short- and long-term pharmacological treatment of ulcerative colitis.
CN102670515A Andrographolide inclusion compound and preparation process thereof The invention discloses an andrographolide inclusion compound and a preparation process thereof, belonging to the technical field of pharmaceutical preparations and relating to a novel andrographolide inclusion compound. The inclusion compound comprises andrographolide and a coating material, wherein the weight ratio of the andrographolide to the coating material is 10:(1-10). After the inclusion compound is adopted, the stability of the andrographolide can be remarkably improved, and the bitter taste is remarkably improved.
EP2503881A1 Fused tricyclic compounds and derivatives thereof useful for the treatment of viral diseases The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
WO2007140385A3 Thiazole compounds as cannabinoid receptor ligands and uses thereof The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specfication, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a and (Rx)n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
CN101732445A Plaster for treating burn and scald The invention relates to a plaster for treating a burn and a scald, which consists of the plaster and packing paper. The plaster is characterized in that: the plaster comprises the following components (in part by weight): 450 to 550g of sesame oil, 200 to 250g of lithargite, 2 to 5g of yellow lead, 3 to 6g of fraxinus chinensis, 10 to 20g of fresh peach twig apex, 20 to 30g of fresh sophora twig apex, and 20 to 30g of fresh willow twig apex. The plaster has the advantages of no need of skin grafting for serious burns and scalds, short treatment course, good analgesic effect, high cure rate, and no scar after healing, and has the characteristics of simple preparation method and no side effects.
WO2014017936A2 Urea compounds and their use as enzyme inhibitors A compound having the following structure: or a pharmaceutically acceptable salt or derivative thereof. The compound may be used in the treatment or prevention of a disorder selected from appetite regulation, obesity, metabolic disorders, cachexia, anorexia, pain, inflammation, neurotoxicity, neurotrauma, stroke, multiple sclerosis, spinal cord injury, Parkinson's disease, levodopa-induced dyskinesia, Huntington's disease, Gilles de la Tourette's syndrome, tardive dyskinesia, dystonia, amyotrophic lateral sclerosis, Alzheimer's disease, epilepsy, schizophrenia, anxiety, depression, insomnia, nausea, emesis, alcohol disorders, drug addictions such as opiates, nicotine, cocaine, alcohol and psychostimulants, hypertension, circulatory shock, myocardial reperfusion injury, atherosclerosis, asthma, glaucoma, retinopathy, cancer, inflammatory bowel disease, acute and chronic liver disease such as hepatitis and liver cirrhosis, arthritis and osteoporosis.
WO2008142860A1 Novel sweetener having sugar-like taste and production method and use of the same [PROBLEMS] To develop a method of producing a novel sweetener containing glucose, fructose and psicose which is produced from glucose-liquid sugar with the use of isomerase and epimerase; a method of using this novel sweetener as a material for foods and drinks; and a novel sweetener whereby obesity caused by eating can be prevented. [MEANS FOR SOLVING PROBLEMS] A novel sweetener (product) sustaining the degree of sweetness and sweetness qualities of a glucose/fructose liquid mixture and yet not causing obesity because of having been obtained by treating glucose-liquid sugar, which is produced in a glucose-liquid sugar production plant, with isomerase and epimerase to thereby form D-psicose and use of the same.
CN101695484A Use of chlorogenic acid in preparing medicament for treating marrow infection The invention provides a use of chlorogenic acid in preparing medicament for treating marrow infection and also provides a pharmaceutical composition containing the chlorogenic acid as the active constituent.
CN102743605A Heat-clearing oral liquid treating pneumonia The invention discloses a heat-clearing oral liquid treating pneumonia. The oral liquid is prepared from the following raw materials by weight part: 5-7 of grilled ephedra, 28-32 of gypsum, 8-10 of stir-fried almonds, 8-12 of raw licorice, 13-17 of polygonum cuspidatum, 13-17 Scutellaria, 8-12 of Fritillaria cirrhosa, 30 of Fructus Trichosanthis, 13-17 of mulberry leaves, 13-17 of mulberry bark, 13-17 of Cortex Lycii, 13-17 of reed rhizomes, 13-17 of forsythia, 13-17 of chrysanthemum, 13-17 of Radix Glehniae, 30-50 of loofah, 30-40 of celery, 40-50 of snow pears, and 13-17 of honey. The invention has a substantial curative effect on pneumonia, and has a total effective rate of 98%.
WO2007091707A1 Pharmaceutical composition for preventing and/or treating bone disease, functional food, health food, pharmaceutical preparation and tooth root-periodontal tissue formation promoting agent containing the composition It is intended to provide a pharmaceutical composition for preventing and/or treating a bone disease which can shorten a period necessary for cure and has high safety and a functional food and the like and a tooth root-periodontal tissue formation promoting agent containing the composition. A pharmaceutical composition for preventing and/or treating a bone disease, a tooth root-periodontal tissue formation promoting agent and the like which contain, as an active ingredient, at least one selected from the group consisting of a compound represented by the formula (I), a physiologically acceptable salt thereof and a hydrate thereof are provided. As a result, the prevention and/or treatment of a bone disease can be carried out safely in a short period of time. Further, the prevention and/or regeneration therapy of a periodontal disease can be carried out effectively.
US20110033384 Chimeric polypeptides and their use The presented invention concerns chimeric molecules that contain a preferential polypeptidic region, consisting of a specific affinity for the binding to specific DNA sequences, of a preferential polypeptidic region consisting of a DNA modifying activity, and this chimeric molecule is capable to cross biological membranes due to the presence of a region that contains delivery activity. The invention contains further the isolated polynucleotides that code for the chimeric molecules of the invention if they are as such entirely or partially of polypeptide nature. In another embodiment, based on the activities of the polypeptides contained in the invention to interfere with key points of the cell-cycle regulation and the cellular checkpoints due to their introduction of DNA double strand breaks, the invention contains various procedures that are characterized by the use of said polypeptides of the invention for cells in vivo and provides an activity for the modification of specific sites of the DNA contained in a cell. The invention also contains procedures that use the chimeric molecules of the invention to screen for new delivery activities or combinations of delivery activities. The invention further provides for the therapeutic use of said compositions as anti-proliferative, anti-neoplastic, antibiotic, antiparasitic or antiviral agents.
US20100130559 Novel phenyl-isoxazol-3-ol derivative The present invention relates to a compound represented by formula (I), which has a GPR120 agonist action and thus is useful for treatment of diabetes mellitus or hyperlipidemia, or a pharmaceutically acceptable salt thereof. In the formula, (AA) represents a phenyl or the like, which may be substituted with a lower alkoxy group or the like; (BB) represents a divalent group or the like, derived by removal of two hydrogen atoms from a benzene which may be substituted with a halogen atom or the like; X represents a spacer having a main chain composed of 1-8 carbon atoms wherein 1-3 carbon atoms in the main chain may be substituted with an oxygen atom or the like; and Y represents a hydrogen atom or the like.
WO2007085567A3 Synergistic compositions for treating hiv Synergistic pharmaceutical compositions for treating or preventing HIV-1 infections comprising anti-CCR5 monoclonal antibodies and CCR5 antagonists, viral fusion inhibitors or viral attachment inhibitors are disclosed. The compositions exhibit significant greater activity than is anticipated from the activity of either component alone. Also provided are methods for treating or preventing HIV-1 using the same.
CN103420986A Compound replacing quinoidines as well as using method and application of compound The invention provides a novel compound replacing quinoidines, acceptable salts of the novel compound on pharmacy and pharmaceutical preparations of the novel compound. The novel compound is used for adjusting the activity of a protein kinase, and an intercellular signal response or an intracellular signal response. The invention meanwhile relates to pharmaceutical compositions comprising the novel compound and a method for treating the highly-proliferative diseases of mammals and particularly treating the highly-proliferative diseases of humans through the pharmaceutical compositions.
US20090131366 Use of Amine-Borane Compounds as Anti-Microbial Agents Use of amine-borane compounds such as amine cyanoboranes and amino carboxy boranes in the treatment of medical conditions associated with pathogenic microorganisms and particularly against drug-resistant microorganisms, in the treatment of fungal and protozoal infections is disclosed. Use of amine-borane compounds for reducing the load of microorganisms in various substrates and products is further disclosed.
CN103462886A Stable levetiracetam injection The invention relates to a stable levetiracetam injection. In particular, the levetiracetam injection provided by the invention comprises levetiracetam, an acidic material, an alkaline material and injection water serving as an injection solvent. The pH value of the levetiracetam injection provided by the invention is 4.5-6.5. The invention further relates to a method for preparing the levetiracetam injection. The fact that the levetiracetam injection provided by the invention has good pharmaceutical properties is unexpectedly found.
WO2007028129A1 Hydroxy substituted 1h-imidazopyridines and methods Hydroxy substituted 1H-imidazo[4,5-c]pyridin-4-amines, with a hydroxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
CA2495527C New sexual-dysfunction-compound-containing rapid-onset pharmaceutical formulations comprising cocoa powder and use thereof A sexual-dysfunction-compound-containing rapid-onset pharmaceutical composition that comprises cocoa powder, process for manufacturing the composition and use of the composition in sexual dysfunction therapy.
US20100099720 Gene Polymorphisms as Sex-Specific Predictors in Cancer Therapy The invention provides compositions and methods for determining the likelihood of gender-specific successful treatment with 5-FU/oxaliplatin or an equivalent of each thereof. The methods comprise determining the genomic polymorphism present in a predetermined region of a gene of interest and correlating the polymorphism to the predictive response. Patients identified as responsive are then treated with the appropriate therapy.
CN102988320A Capecitabine dispersible tablet and preparation method thereof The invention discloses a capacitabine dispersible tablet and a preparation method thereof. The formula of the dispersible tablet is as follows: the proportion of a main drug of capacitabine ranges from 70%-80%; the proportion of an adhesive of polyvinylpyrrolidone K30 ranges from 3%-7%; the proportion of a disintegrating agent of cross-linked sodium carboxymethyl cellulose ranges from 3%-7%; and the proportion of a filling agent of microcrystalline cellulose ranges from 10%-20%.
CN101584685A Medicine composition for regulating blood fat The invention relates to a medicine composition for regulating blood fat, belonging to the field of medicine. The medicine composition for regulating the blood fat comprises the following compounds by weight percent: 10-35 percent of 3,7-dihydroxy-2,4,6-trimethoxy phenanthrene, 10-35 percent of1-(2,7-dihydroxy-4,6-dimethoxy phenanthrene)-2,7-dihydroxy-4,6-dimethoxy phenanthrene, 10-35 percent of 7-hydroxyl group-2,6-dimethoxy-1,4-phenanthrenequinone, 10-35 percent of kaempferol-3-O-beta-D-glucopyranoside, 10-35 percent of kaempferol-3-O-beta-rutinoside and 10-35 percent of rutin. The invention has the advantages that the ingredients of the medicine composition are all obtained by being extracted and separated from the aboveground part of dioscorea nipponica makino; the medicine composition belongs to natural products and has high capability for regulating the biological activity of the blood fat; and an optimal proportion of ingredients of compositions for treating hyperlipoidemia.
CN1872185A Granula of possessing function for improving sleeping A medicine in the form of particles for improving the quality of sleeping is proportionally prepared from glycine, extract of wild jujube, oligoxylose, bony calcium phosphate, malt dextrin, mannose, essence, and pantothenic acid, VB1, VB2 and VB6.
CN102091096A Artificial cow-bezoar and chlorphenamine maleate granules containing bezoar cultured in vitro and preparation method thereof The invention relates to artificial cow-bezoar and chlorphenamine maleate granules containing bezoar cultured in vitro and a preparation method thereof. Based on weight part, the artificial cow-bezoar and chlorphenamine maleate granules are prepared from 5 parts of bezoar cultured in vitro, 125 parts of paracetamol, 0.5 part of chlorphenamine maleate, and a proper amount of cane sugar and essence. The preparation method is to mix and grind medicines by an equal gradual increase process and granulate the ground materials. The invention is characterized in that: the replacement of artificial bezoar by bezoar cultured in vitro can reduce the side effects of vomit and icterus caused by over high free bilirubin content in the artificial bezoar; and the mixing and grinding by the equal gradual increase process can effectively disperse the active ingredients of the medicine and reduce the side effect caused by non-uniform medicine content.
EP1286667B1 Composition for the treatment and/or the prevention of osteoporosis and/or inflammatory joint diseases Compositions and pharmaceutical compositions are described which comprise: a component A comprising one or more flavonol glycosides, a component B comprising one or more tetrahydrofolic acid compounds, a component C comprising one or more calcium supplements, and a component D comprising one or more magnesium supplements. Methods of using such compositions and pharmaceutical compositions to treat and/or prevent osteoporosis and/or an inflammatory joint disease are also described.
CN103142558A Diclofenac sodium dual-release enteric-coated preparation, as well as preparation method and control method thereof The invention relates to a diclofenac sodium dual-release enteric-coated preparation, as well as a preparation method and a control method thereof. The diclofenac sodium dual-release enteric-coated preparation comprises the following components in percentage by weight: 11%-44% of microcrystalline cellulose, 2%-5% of ethyl cellulose, 3%-10% of povidone, 1%-6% of Eudragit S100, 2%-16% of Eudragit RL PO, 2%-12% of Eudragit RS PO, 1.5%-12% of tributyl citrate, 0.01%-0.1% of sodium hydroxide, 0.05%-1% of propylene glycol, 6%-15% of talc powder, 0.1% of silicon dioxide, 0.3% of titanium dioxide and 0.3% of dimethyl silicone oil, A and B pills with two release mechanisms are respectively prepared, and double-layer tablets, capsules or granules are prepared, wherein a prepared intermediate product has the laser spectral band pass of 5.0nm, the transmission spectral band pass of 10.0nm, the excitation wavelength of 340nm and the fluorescence intensity of 330-380 under the condition that the transmission wavelength is 510nm. The quality of the diclofenac sodium dual-release enteric-coated preparation disclosed by the invention is in line with the standard, and quality control is performed before production, so that rework can be reduced, the production cost can be saved, the energy consumption can be reduced and the production efficiency can be improved.
US20130023543 Human protein tyrosine phosphatase inhibitors and methods of use The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.
CN101505741A A cyclohexane polyalcohol formulation for treatment of disorders of protein aggregation The invention provides formulations, dosage forms, and treatments comprising cyclohexane polyalcohol compounds that provide beneficial pharmacokinetic profiles in the treatment of a disorder and/or disease including a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence. In aspects of the invention, a dosage form is provided comprising an amount of a cyclohexane polyalcohol compound suitable for administration to a subject to provide a therapeutically effective concentration of the compound in plasma, brain and/or cerebral spinal fluid and a pharmaceutically acceptable carrier, diluent or excipient. The formulation can be administered in a dose of 500, 1000, 2000, 3500, 5000 or 7000 mg of cyclohexane polyalcohol compound to achieve a mean plasma concentration profile having a mean AUC0-INF in [mu].h/mL of, respectively, 43+-20%, 130+-20%, 215+-20%, 467+-20%, 507+-20% or 885+-20%, and having a mean Cmax in [mu]mL of, respectively, 5.8+-20%, 17+-20%, 33+-20%, 75+-20%, 110+-20% or 155+-20%.
EP1495009B1 Cyanamides useful as reversible inhibitors of cysteine proteases Compounds according to the following formula (I): wherein the variables Q and Rl to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.
EP1024835B1 J-chain and analogues as epithelial cell targeting conjugates Targeting molecules for use in delivering biological agents to non-polarized epithelial cells are disclosed. Upon delivery, the biological agent(s) are lethal to the epithelial cell. The targeting molecules may be used, for example, for the eradication of metastatic epithelial cells.
CN102626398A Pantoprazole sodium enteric-coated tablet and preparation method thereof The invention provides a pantoprazole sodium enteric-coated tablet, which consists of the following components in parts by weight: 1 part of a pantoprazole sodium plain film, 0.1-0.5 part of an isolating layer and 0.5-1 part of an enteric-coated layer, wherein the isolating layer consists of hydroxypropyl methylcellulose and an alkali in the weight part ratio of 1:5-5:1; and the enteric-coated layer is prepared from 0.5-1 part of acrylic resin. The invention provides a preparation method of the pantoprazole sodium enteric-coated tablet. Parameters such as spray speed, spray pressure, the rotating speed of a coating pan and the like are improved through process parameters of the isolating layer, an enteric liquid and a coating, so that the prepared pantoprazole sodium enteric-coated tablet has high acid tolerance and dissolution rate, the acid tolerance of a finished product is over 90 percent, the dissolution rate is over 75 percent, and the pantoprazole sodium enteric-coated tablet is accordant with and superior to the requirements of the Chinese Pharmacopoeia on the enteric tablet. The product has the advantages of stable quality, convenience for storing and transporting and contribution to clinical application. The method is simple, is suitable for industrial production, and has high application value.
US20110280860 Pharmaceutical compositions comprising monoterpenes The present invention provides a process for purifying a monoterpene or sesquiterpene having a purity greater than about 98.5% (w/w). The process comprises the steps of derivatizing the monoterpene (or sesquiterpene) to produce a monoterpene (or sesquiterpene) derivative, separating the monoterpene (or sesquiterpene) derivative, and releasing the monoterpene (or sesquiterpene) from the derivative. Also encompassed by the scope of the present invention is a pharmaceutical composition comprising a monoterpene (or sesquiterpene) having a purity greater than about 98.5% (w/w). The purified monoterpene can be used to treat a disease such as cancer. The present monoterpene (or sesquiterpene) may be administered alone, or may be co-administered with radiation or other therapeutic agents, such as chemotherapeutic agents.
US20080267940 Using protamine to precipitate fibrinogen from whole blood; wound healing agent The present invention is drawn to concentrated fibrinogen compositions and associate methods and use thereof. The concentrated fibrinogen compositions can be produced by adding a sufficient amount of a cationic agent, such as protamine, to a fibrinogen containing fluid to cause the fibrinogen to form a fibrinogen precipitate; collecting the fibrinogen precipitate by a collection means, such as centrifugation; and suspending or solubilizing the fibrinogen precipitate in a liquid vehicle to form a concentrated fibrinogen composition. The concentrated fibrinogen compositions can be incorporated into systems for making fibrin glues and be used in treating wounds.
WO2010040992A1 Quinoline derivatives having dp and / or crth2 receptor activity A compound of formula (I) for medicinal use: R1, R2, R3, R4 and R5 independently represent hydrogen, halogen, -S(O)nR6, -S(O)2NR7R8, -NR7S(O)2R6 -NR7R8, -NR7COR6, -CONR7R8, -COR6, - NO2, -CN, -OR7, C1-C6alkyl or C3-C7cycloalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; R6 is C1-C6alkyl or C3-C7cycloalkyl, optionally substituted by one or more fluoro atoms; R7 and R8 independently represent hydrogen, C1-C6alkyl or C3-C7cycloalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; A is -O-, -S(O)n, -CR9R10, -NR11 or -C(O); R9 and R10 independently represent a hydrogen, fluoro or C1-C6alkyl; R11 and R12 independently represent hydrogen or C1-C6alkyl; B is -C(R9R10)C(R9R10)- or C(R11)=C(R12); and when A is -CR9R10, B may additionally be -OCR9R10, -NR11CR9R10 or -S(O)nCR9R10; W is C1-C6alkyl optionally substituted by one or more substituents independently selected from fluoro, aryl, heteroaryl or C3-C7cycloalkyl, the latter group being optionally substituted with one or more fluoro atoms; and X is a carboxylic acid group, a tetrazolyl group, or a group of formula -CONHS(O)2R13 or -S(O)2NHCOR13; R13 is aryl, heteroaryl, C1-C6alkyl or C3-C7cycloalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and n is 0, 1 or 2.
WO2010124856A1 Use of 1-phenyl-3-dimethylaminopropane compounds for treating rheumatoid pain The invention relates to the use of l-phenyl-3- dimethylaminopropane compounds for the production of medicaments for treating rheumatoid, preferably rheumatoid arthritic, very preferably chronic rheumatoid arthritic pain.
CA2660939A1 Pharmaceutical compositions for the treatment of fungal infections Synergistic combinations of a squalene epoxidase inhibitor and a leucyl-tRNA synthetase inhibitor are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin or nail plays a role, such as atopic dermatitis, acne vulgaris, seborrhoeic dermatitis, rosacea or onychomycosis, and in situations of fungal resistance.
WO2010071846A2 Compounds for treating neuropsychiatric conditions Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of neuropsychiatric conditions.
WO2014030743A1 Heterocycic compound Provided is a compound which has an excellent FLAP inhibitory activity and is useful as a prophylactic or therapeutic agent for arteriosclerosis and the like, or a salt of the compound. The present invention relates to a compound represented by formula (I) or a salt thereof. (In the formula, the symbols are as defined in the description.)
US20130331362 Ophthalmic Solution For Absorbing Ultraviolet Radiation and Method For Absorbing Ultraviolet Radiation An ophthalmic solution is provided. The ophthalmic solution includes an ultraviolet-A absorber and an ultraviolet-B absorber. The ophthalmic solution has a viscosity of between about 1 and 100 cps. The ophthalmic solution can be used to absorb ultraviolet radiation in the eye.
CN101606941A Injection liquid for treating nocardia seriolae infection of dog and preparation method thereof The invention discloses an injection liquid for treating nocardia seriolae infection of a dog and a preparation method thereof, aiming at providing an injection liquid which has fast effect for treating nocardia seriolae infection of the dog, addresses both the symptoms and root causes, reduces the time and dosage of taking drug, and a preparation method thereof. Each 100L of injection liquid comprises: 2 to 15kg of sulfamethoxydiazine sodium, 0.4 to 3kg of trimethoprim, 2 to 15kg of aminopyrine, 0.05kg of bethanechol chloride, 0.05kg of dexamethasone sodium phosphate, 0.01kg of EDTA-2Na, 0.2kg of sodium bisulfite, 20kg of dimethyl acetamide, 20kg of propylene glycol, 10kg of 95% alcohol and the balance of water for injection. The injection liquid adopts sulfamethoxydiazine sodium as an antibacterial agent, matches sulfonamides special synergistic agents, aminopyrine as febrifuge, the bethanechol chloride promoting gastrointestinal dynamic, and glucocorticoid dexamethasone sodium phosphate functions of resisting inflammation and clearing away toxicity, can fast disinfect harmful bacteria, treating clinical symptoms of representation of the patient dog, restore food sampling, is beneficial to recovery, and has convenient use.
US20110275679 Flupirtine hydrochloride maleic acid cocrystal The invention relates to crystalline forms of flupirtine, particularly to 1:1 flupirtine hydrochloride maleic acid cocrystal. The preparation and characterization of 1:1 flupirtine hydrochloride maleic acid cocrystal is described. The invention also relates to the therapeutic use of the flupirtine hydrochloride maleic acid cocrystal to treat nervous system disorders, pain disorders, and musculoskeletal disorders and to pharmaceutical compositions containing the cocrystal.
US20120184514 Vitamin d compounds and methods for preparing same An air-stable, high-melt 1a-hydroxy-vitamin D3 compound, methods for preparing an animal feed composition, methods of preparing 1α-hydroxy-vitamin D3, methods of enhancing phytate phosphorus and calcium utilization, and an animal feed regime are provided.
CN100999518A Voriconazole derivate and preparation process thereof This invention involves Voriconazole derivatives. The invention also involves Voriconazole derivatives preparation methods, including the following steps : 2 - (5-fluoro-4-yl) acetate and ethanol for esterification, generate 2 -(5-fluoro-4-yl) ethyl acetate, in alkaline conditions takes reaction with methylation agent, generate 2 - (5-fluoro-4-yl) ethyl propionate; hydrolysis of 2 - (5-fluoro-4-yl) propionic acid, through split gain S-2 - (5-fluoro-4-yl) propionic acid; for chlorination to gain S-2 - (5-fluoro-4-yl) propionyl chloride; occurred Friedel-Crafts reaction, generating S-1 - 2, 4-difluoro-2 - (5-fluoro-4-yl) acetone; with 1-methyl - 1-H-1 ,2,4 - triazol under alkali conditions to take reaction to gain voriconazole and the series of voriconazole derivatives. The methods described in this invention has short routes, only use of a pair of enantiomers separation, the overall yield has been greatly improved, is a simple and easy method for synthesis of voriconazole and its derivatives.
US7306950 Composition and use of substances for stabilising amino acids containing sulphur The invention relates to a composition for the stabilization of sulphur-containing amino acids and/or for the inhibition of the continuous formation of sulphur-containing amino acids in withdrawn blood, to the use of suitable substances and compositions therefor as well as optionally for the determination of sulphur-containing amino acids in blood, to a process for these purposes, as well as to a blood collecting device applied appropriately to these processes.
WO2013068785A1 Indanone and indandione derivatives and heterocyclic analogs The invention relates to indanone/indandione derivatives and heterocyclic analogs of Formula (I) wherein Ar1, A, B, L1, Y, Z, and (R1)n n are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as NPS receptor antagonists.
WO2014142644A1 Antiviral activity of baicalein against japanese encephalitis virus The present invention provides an antiviral medicament for treating Japanese Encephalitis Virus (JEV) infection comprises a natural flavonoid compound namely baicalein. In the present invention, antiviral activity of baicalein was evaluated against JEV replication in African green monkey kidney cell line (Vero). Anti-JEV activities of baicalein were examined at different stages of JEV replication cycle. The effects of baicalein on virus replication were determined from Foci Forming Unit Reduction Assay (FFURA) and quantitative RT-PCR.
US20130261085 Method of improving response to chemotherapy by administering a phospholipid together with chemotherapeutic agents, and formulations therefor Methods and formulations for improving efficacy of chemotherapeutic treatment. The formulation includes at least one chemotherapeutic agent and at least one phospholipid or a material comprising the same. The phospholipid facilitates entry of the at least one chemotherapeutic agent into cells of an afflicted individual. A sufficient dosage of a blood-thinning agent is optionally included to mitigate risk of developing blood clots attributable to administration of the chemotherapeutic agent(s). The chemotherapeutic agent(s) and the phospholipid(s), or the material containing the phospholipid(s), are administered in any order but in sufficient time proximity to one another such that the effect of the phospholipid(s) of facilitating entry of the chemotherapeutic agent(s) into the cells at least partially overlaps with the therapeutic effect of the chemotherapeutic agent(s).
EP1737467A4 Method and composition for treatment of skin conditions A method for treating dermatological conditions as eczema, seborrheic dermatitis, psoriasis and allergic skin reactions such as hives, skin irritations, poison ivy, poison oak, and the like. The method involves applying to the affected area of the skin a few drop of a combination of pheniramine maleate and either naphazoline HCL or phenylephrine HCL and then applying to the same affected area a topical corticosteroid cream, ointment or lotion. The preferred ratio is approximately one drop of solution for every approximately 0.1 grams of topical corticosteroid cream applied to each patch of skin affected with any of he dermatological conditions.
CN103356509A Film agent containing zolpidem serving as main active component The invention discloses a film agent containing zolpidem serving as a main active component and relates to a film agent which contains zolpidem serving as a main active component and is dispersed and dissolved in the oval cavity, as well as the in vitro property of the film agent. The preparation is attractive in appearance, convenient to carry, simple to take and quick to disintegrate, can be disintegrated in the oral cavity without water, and is particularly suitable for the old, children and patients hard to swallow.
US6914053 5-(hydroxymethyl)- or aminocarbonyl-2-(6-(alkoxyamino)-2-(optionally substituted ethynyl)purin-9-yl)tetrahydrofuran-3,4-diol derivatives; treatment of ischemia, asthma, leukopenia and neutropenia, cancer and inflammation. Disclosed are novel adenosine A3 receptor agonists of Formula I: wherein: R is hydrogen or lower alkyl; R1 is optionally substituted lower alkoxy or optionally substituted cycloalkyloxy; R2 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted trialkylsilyl; and R3 is hydroxymethyl or R4R5NC(Q)—; in which R4 and R5 are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl.
WO2014163210A1 [11 c] and [18f] labeled 1,3-diphenyl-5-(pyrimidin-2-yl)-pyridin-2(1 h)-one derivatives and their use for pet imaging of the ampa receptor A compound selected from the group consisting of compounds represented by the formulas below or pharmaceutically acceptable salt thereof is useful in PET imaging for AMPA receptor.
CN102961352A Preparation method of doxazosin mesylate sustained-release dropping pill for treating hypertension and prostatic hyperplasia The invention belongs to the technical field of pharmacy, and particularly relates to a preparation method of doxazosin mesylate sustained-release dropping pill for treating hypertension and prostatic hyperplasia. Based on doxazosin mesylate tablets, the invention employs existing dropping pill preparation technology to prepare the doxazosin mesylate sustained-release dropping pill. Compared to the prior art, the invention is the supplement for the defects of existing drug form production, and provides a drug, which has advantages of high bioavailability, rapid effectiveness, long-acting effect, little toxic or side effect, high drug content, small and accurate dosage, convenient usage, low price and convenience for carrying.
US20050059594 Administering macrophage derived factor; oncomodulin Methods and compositions for producing a neurosalutary effect in a subject, such as modulating neuronal survival and/or regeneration in a subject, are provided. Pharmaceutical and packaged formulations are also provided.
WO2013114232A1 Process for preparation of crystalline form l of ilaprazole The present invention relates to the process for preparation of crystalline form L of ilaprazole comprising steps of: i) heating the mixture of ilaprazole in aliphatic ketone containing tertiary organic amine, ii) cooling the mixture, iii) optionally seeding with form L and iv) isolating solid. The present invention further relates to the novel crystalline form L of ilaprazole characterized by a powder X-ray diffraction pattern having peaks at 6.60, 8.24 and 16.05 ± 0.2 degree 28 and an infra-red spectrum having peaks at 1417 and 1434 ± 5 cm-1.
US20110237641 Substituted pyrazoles, compositions containing these, method of production and use The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
CN102949523A Medicinal composition used for relieving visual fatigue and preparation method of capsules thereof The invention discloses a medicinal composition used for relieving visual fatigue and a preparation method of capsules thereof. The medicinal composition comprises the following components in parts by weight: 25 parts of semen cassiae, 20 parts of chrysanthemums, 15 parts of wolfberry fruit, 20 parts of cornus officinalis, 10 parts of procyanidine and 10 parts of taurine. The medicinal composition disclosed by the invention is expected to achieve the effect of relieving the visual fatigue, is processed by using the semen cassiae, the chrysanthemums, the wolfberry fruit, the cornus officinalis, the procyanidine and the taurine as the main raw materials and adopting a scientific and reasonable production technology, and has the advantages of clear function, controllability in quality and safety in taking. The preparation method of the medicinal composition, which is disclosed by the invention, is simple, and the medicinal composition can be prepared only by using conventional equipment.
WO2013038407A1 Amorphous form of dolutegravir The present invention provides an amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.
WO2010065802A2 Substituted pyrrolidine or imidazolidine melanocortin receptor-specific compounds A compound of the formula I, where R1, R2a, R2b, R3, L1, L2, Q, J, X, Y, Z, m and n are as defined, or an enantiomer, stereoisomer or diastereoisomer thereof, or a pharmaceutically acceptable salt thereof, and the use thereof in the treatment of diseases, syndromes and conditions mediated through melanocortin receptors.
US20060018962 Sustained release formulation of tramadol This invention relates to sustained release oral dosage forms comprising tramadol or a salt thereof dispersed in a matrix, wherein said matrix comprises xanthan gum.
CN102070532A Anti-tumor medicament structure The invention provides a novel anti-tumor medicament structure which is shown by a structural general formula (I). In the formula, R1 to R5 are independently selected from H, NO2, OH, halogen and OCH3. The medicament has a simple and convenient synthesis method, and molecules comprise nitroxide free radical structure units, so the anti-tumor medicament structure can effectively suppress proliferation of liver cancer, stomach cancer, breast cancer and ovarian cancer cells.
CN103145657A 17-hydro-9-dehydroandrographolide compound and its preparation method and use in drug preparation The invention discloses a 17-hydro-9-dehydroandrographolide compound or its salt, and its preparation method and use in drug preparation. The 17-hydro-9-dehydroandrographolide compound or its salt has effects of bringing down a fever, diminishing inflammation and resisting viruses. The 17-hydro-9-dehydroandrographolide compound or its salt does not change chemical properties of andrographolide, has characteristics of good water-solubility, high thermostability and low hemolysis, and guarantees the pharmacological activity of an andrographolide all-natural drug to the maximum degree. Medical and pharmaceutical researchers cannot know the above uses of sodium 17-hydro-9-dehydroandrographolide in advance without related experiments.
EP2146712A1 Aryl heterocyclic cgrp receptor antagonists Compounds of formula I: I (wherein variables A1, A2, B, m, n, J, X, R4, G1, G2, G3 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
WO2006090743A1 1-(2h)-isoquinolone derivative Disclosed is a compound represented by the formula (1) below, a prodrug thereof, or a pharmaceutically acceptable salt of either of them. Also disclosed are a pharmaceutical product, pharmaceutical composition and the like containing such a compound which are useful for effectively treating and preventing proliferative diseases such as cancers. (1) [In the formula, X represents an optionally substituted aryl group or heteroaryl group; Cy represents an optionally substituted 4-7 membered single heterocyclic ring or 8-10 membered fused heterocyclic ring; and Z represents O, S or NRa.]
US20100286253 Method for treating ocular neovascularization Methods are provided for the treatment of ocular neovascularization by increasing, in an individual afflicted with ocular neovascularization, in vivo concentrations of an endostatin protein in the ocular tissues of the individual to an ocular neovascularization inhibiting effective amount, where the endostatin protein has anti-ocular neovascularization activity in vivo.
CA2315117C Heterocyclic ether and thioether compounds useful in controlling chemical synaptic transmission Novel compounds having formulas (I), (II) or (III) or pharmaceutically-acceptable salts or prodrugs thereof, which are useful for controlling synaptic transmission; to therapeutically-effective pharmaceutical compositions of these compounds; and to the use of said compositions to controlling synaptic transmission in human or veterinary patients.
WO2007075808A2 Methods for preventing and/or treating a cell proliferative disorder The present invention relates to methods for preventing and/or treating the growth and/or metastasis of a cell proliferative disorder. In particular, the methods include use of a protease activated receptor-1 (PAR-1) inhibitor.
EP1982696A1 Gel for treating wounds The antiseptic gel is made of 16-20 wt.% of poloxamer 407 basis. Additionally, 0.01-2.0 or 0.05-0.1 wt.% of octenidine or polihexanide as active substance, 58 wt.% of water, and glycerin are also provided. The gel has viscosity increase of 20 Pas in 18-25o?C temperature range within a range of 2o?C. An independent claim is also included for a method for production of an antiseptic gel, which involves carrying out the production of the gel under aseptic conditions. - ACTIVITY : Vulnerary. - MECHANISM OF ACTION : None given.
CN103204771A Naphthoquinone or naphthalenone compounds and preparation methods thereof and applications of drugs thereof The invention belongs to the field of pharmaceuticals, relating to naphthoquinone or naphthalenone compounds with structural formulas shown in formula (I) or formula (II), and preparation methods thereof and applications thereof in pharmaceuticals, particularly the application in treatment of tumors. The naphthoquinone or naphthalenone compounds of the invention can be obtained by a synthesis method or by an extraction and separation method from plants. Results of anti-tumor activity tests show that the obtained naphthoquinone or naphthalenone compounds can significantly inhibit tumor cell activity of different types of lung cancers. The naphthoquinone or naphthalenone compounds can be prepared to be drugs or drug combinations to be systemically or topically delivered by using a carrier or an excipient for the treatment of lung cancers.
CN102920663A Famciclovir sustained-release pellet, preparation method and application thereof The invention provides a famciclovir sustained-release pellet, a preparation method and an application thereof. The famciclovir sustained-release pellet provided by the invention is composed of a blank pellet core used as a core, a main drug layer containing famciclovir and coating the pellet core, and a sustained-release coating layer coating the main drug layer; the weight of polymer contained in the sustained-release coating layer is 8-15% of the total weight of the blank pellet core and the main drug layer. The famciclovir sustained-release pellet is prepared by a spraying method. According to the famciclovir sustained-release pellet provided by the invention, not only the high drug release rate of the famciclovir sustained-release pellet in an acidic medium is significantly inhibited, but also the final complete release is not influenced; and the following release degree scopes can be realized: 10-30% (1.5 hours), 30-70% (3 hours), and not less than 90% (8 hours).
CN103417471A Lipoxin emulsifiable paste for curing skin inflammations such as eczema Emulsifiable paste, which is used for curing skin inflammations such as eczema, is externally used on the skin, and contains lipoxin, is prepared by following steps: dissolving lipoxin A4 methyl ester in 1% dimethyl sulfoxide, and then adding non-ionic substrate so as to obtain the emulsifiable paste. The lipoxin emulsifiable paste is mainly used for eczema, but can be applied to other skin allergic diseases too. The curative effect of the lipoxin emulsifiable paste is the same as that of sugar-free cortical hormone emulsifiable paste, but the sugar-free cortical hormone emulsifiable paste has side effects which cause the symptoms of skin incontinentia pigmenti, skin atrophy, and angiotelectasis. The lipoxin emulsifiable paste has no systemic side effects.
CN103432132A Pridinol mesylate diclofenac sodium injection and preparation method thereof The invention discloses a pridinol mesylate diclofenac sodium injection. The injection comprises the following components in every 100mL: 0.2g of pridinol mesylate, 2.5g of diclofenac sodium, 15-27mL of PEG400 (polyethylene glycol), 4-6mL of benzyl alcohol, 0.6g of mannitol, 0.3g of sodium pyrosulfite, a sodium hydroxide solution used for regulating the pH to 8.0-8.6, and the balance of injection water. The injection water and PEG400 are of a mixed solvent, and assisted by benzyl alcohol to solve the technical problem that pridinol mesylate and diclofenac sodium are easily separated out in the preparation process; sodium pyrosulfite and mannitol are combined for resisting oxidation, so that the problem that the diclofenac sodium is not stable in a water solution can be solved; the injection is advanced in prescription, simple in preparation process, low in cost, stable, safe and effective, is suitable for intramuscular, subcutaneous or intravenous injection delivery, and is advantageous to fulfill the requirement for clinical treatment.
CN101897848A Medicament for treating venomous snake bite The invention discloses a method for preparing a medicament for treating a venomous snake bite. The method is implemented by a technical scheme which comprises: putting raw materials of clematis root, weeping forsythia and pinellia tuber between two tiles; closing and placing the two tiles into a drying box; heating for 20 to 30 minutes at the temperature of between 100 and 120 DEG C; taking the raw materials out and decocting and boiling the raw materials for 15 minutes; filtering to obtain decoction; adding water again and decocting and boiling the raw materials for 20 minutes; removing dregs; and uniformly blending decoction obtained at two times to obtain the medicament for treating the venomous snake bite, wherein the medicament is taken by several times. Simultaneously, realgar and trogopterus dung are ground into powder together, and the powder is applied onto wounds after being mixed with good wine. The method can improve the curative effect obviously.
CN102775428A Pyrazole alkanol-copper complex and preparation method and application thereof The invention discloses a pyrazole alkanol-copper complex and a preparation method and application thereof. The molecular formula of the pyrazole alkanol-copper complex is CuLBr 4H2O, wherein the L is 1,3-di (3-(2-pyridine) pyrazole)-2-propyl alcohol and has antineoplastic activity. The preparation method of the pyrazole alkanol-copper complex includes firstly synthetizing DMF-DMA (dimethylformamide dimethyl acetal) with 2-acetylpyridine to obtain 1-(2-pyridyl)-3-dimethylamino-2-acrylketone, synthetizing the 1- (2-pyridyl) -3-dimethylamino- 2-acrylketone with hydrazine hydrate to obtain 3-(2-pyridine) pyrazole, synthetizing the 3-(2-pyridine) pyrazole with 1,3-dichloro-2-propyl alcohol to obtain 1,3-di (3- (2-pyridine) pyrazole)-2-propyl alcohol, and synchronizing the 1,3-di (3- (2-pyridine) pyrazole)-2-propyl alcohol with cupric bromide-methyl alcohol solution to obtain the pyrazole alkanol-copper complex having antineoplastic activity. The preparation method is reasonable in design, simple to operate, high in yield and beneficial for practical production.
EP2709615A1 Monoclinic crystalline form of asenapine maleate with a specific particle size distribution A monoclinic crystalline form of asenapine maleate is described, which is characterized in that it is not micronised and has a particle size distribution characterized by a d90 of 40 μm or less. A process for the preparation of a monoclinic crystalline form of asenapine maleate is also described, the process comprising the following steps: a) providing a mixture of monoclinic asenapine maleate and an organic solvent which, under the conditions of the process, acts as an antisolvent; b) stirring the mixture at a temperature between 15 and 60°C; and c) collecting the crystals, wherein the organic solvent is selected from alcohols, ketones, ethers, esters, hydrocarbons or mixtures thereof.
US20100184690 Combined Use Of A GLP-1 Compound And A Modulator Of Diabetic Late Complications Methods and uses for treatment of diabetic late complications comprising administration of a GLP-1 compound and a modulator of diabetic complications.
CN101791368A Edible fungi combined polysaccharide health-care capsule for males The invention discloses an edible fungi combined polysaccharide health-care capsule for males, which comprises the following components in percentage by weight: 20 to 30 percent of lentinan, 50 to 80 percent of lentinan by-product, 20 to 60 percent of white fungus polysaccharide, 20 to 50 percent of by-product of white fungus polysaccharide, 50 to 80 percent of agaricus blazei polysaccharide, 20 to 50 percent of by-product of agaricus blazei polysaccharide, 10 to 15 percent of leek, and 5 to 15 percent of dried silkworm fine powder. The combined polysaccharide health-care capsule of the invention mainly comprising the lentinan, white fungus polysaccharide and agaricus blazei polysaccharide can be preserved at normal temperature, and can improve the secretion level of gonadal hormone, improve the sexual function and sperm activity of the males, promote the gonadal development and growth, repair the damaged tissues and cells, and improve the vigor of life; and have the functions of tonifying middle-Jiao and Qi, warming and activating meridian, and strengthening waist and invigorating kidney.
CN101239018A Multilayer copolymerized compound membrane soft bagged inosine in sodium chloride injection composition and its manufacturing method The invention relates to a multi-layer co-extrusion compound film inosine sodium chloride injecta composite packaged by soft bag: every 100 ml inosine sodium chloride injecta composite contains 0.6g plusing or subtracting 0.05g inosine, 0.9 plusing or subtracting 0.05g sodium chloride, 0.1g plusing or subtracting 0.02g D-gluconic acid-delta-lactone; in a hundred-level cleaning area, after adopting a multi-layer co-extrusion compound film and a plastic transfusion vessel joint to heat, the inosine solium chloride injecta composite is filled and sealed with a plastic transfusion vessel pull-tab type seal cover, to obtain multi-layer co-extrusion compound film inosine sodium chloride injecta composite packaged by soft bag. The preparation method is: inosine or the mixture of inosine and D-gluconic acid-delta-lactone is added by water for injection, adding sodium chloride after mixing and being filtered by microporous filtering film to obtain inosine sodium chloride injecta composite; after adopting a multi-layer co-extrusion compound film and a plastic transfusion vessel joint to heat, the inosine solium chloride injecta composite is filled and sealed with a plastic transfusion vessel pull-tab type seal cover, then through sterilization to obtain the composite of the invention.
US20100184837 Small-molecule nucleotide aptamer for hepatitis C virus, preparation method and use thereof A DNA aptamer specific for HCV having a nucleotide sequence as shown in SEQIDNO.1-29, and a method of preparing the same including the steps of: (1) constructing a single-stranded DNA library; (2) constructing a double-stranded DNA library; (3) screening by SELEX; (4) amplifying by PCR; (5) cloning and sequencing; and (6) testing the effect from cellular level in vitro. The DNA aptamer can be used directly as medication and diagnostic reagent for detection, prevention, and treatment of hepatitis C. A method for detection of HCV infection is also provided.
WO2012175715A1 Piperazine derivatives, methods for preparing same, and uses thereof in the treatment of insulin resistance The invention relates to a compound of formula (I), where R1, R2, R7, m, n, and L1 are as defined in claim 1, and to the methods for preparing same, to the pharmaceutical compositions containing same, and to the uses thereof in the treatment of diseases associated with insulin resistance syndrome.
WO2008009909A1 Pteridimones as modulators of polo-like kinase There is provided a compound of formula (I) : or a pharmaceutically acceptable salt thereof. Processes for the manufacturing thereof and uses in therapy.
CN101199612A Tincture medicament for treating II degree frozen The invention relates to a Chinese drugs preparation, namely a tincture medicament for treating II degree frostbite. The medicament is made by following materials by weight: 30g of angelica, 30g of red sage root, 30g of acontum fischeri, 30g of rose, 30g of monthly rose, 15g of hippocampus, 10g of cantharis, 20g of magnet and 1000 ml of 75 percent alcohol. The invention has advantages of novel formula, low cost, easy preparation and remarkable effect.
CN103330769A Spray agent for treating epilepsy The invention provides a spray agent for treating epilepsy, which comprises the following raw materials in parts by weight: 8 parts of borax, 7-9 parts of cicada slough, 7-9 parts of radix achyranthis bidentatae, 7-9 parts of uncaria, 7-9 parts of artemisia sylvatica, 5-7 parts of bezoar, 4-6 parts of antelope horn and 1-2 parts of musk. The spray agent has the benefits that the spray agent is administrated directionally and absorbed percutaneously, treats an internal illness by external treatment, and is convenient to carry and convenient to use; stimulation on a stomach of a patient and toxic and side effects on a liver are avoided; effective components in the spray agent can be free from damage of digestive juice, and effect reduction due to a first pass effect of the liver can also be avoided, so that the spray agent can be absorbed by the patient more quickly and better; after the spray agent is sprayed at the top of a head in a spot manner for 3-12min, symptoms of oxygen deficit, paradoxical discharge of a brain wave, hyperpyrexia and the like can be alleviated; the spray agent becomes effective quickly; the epilepsy can be cured after 3-6 months; and the spray agent is safe, efficient, exact in drug effect and high in cure rate, starts a novel administration mode, and has initiativeness.
WO2012177893A3 Trpm8 antagonists and their use in treatments Compounds of Formula I are useful as antagonists of transient receptor potential melastatin 8 (TRPM8). They are useful in treating disorders and conditions such as migraines and neuropathic pain. Compounds of Formula I have the following structure: where in particular X1 and X 2 may be C or N, and R1 is a ring.
CN1742748A Methy cobalamine dispersion tablet and preparing method The present invention provides a mecobalamin dispersing tablet and its preparation method. Every 1000 tablets contain the following components: mecobalamin 0.5g, carboxy methyl starch sodium 5-10g, low-sustituted hydroxypropyl cellulose 15-30g, microcrystalline cellulose 50-65g, polyvidone 1-3g, micropowder silican gel 5g, stervioside 5g, magnesium stearate 1g and talucm powder 1g.
CN103396397A Lenalidomide derivative and use thereof as medicine The invention relates to a lenalidomide derivative and a use thereof as a medicine, and in particular relates to a compound shown as a formula (I), a solvate, a hydrate, a stereoisomer or pharmaceutically acceptable salt thereof. The invention further relates to a pharmaceutical composition comprising the compound, and the use of the compound in preparing medicines for preventing or treating malignant tumors, in particular malignant tumors in the blood-lymphatic system. Compared with lenalidomide, the compound provided by the invention has a longer half-life period and can be used for preparing long-acting preparations.
CA2695435A1 Combination of nitroderivatized steroid and bronchodilator for treating respiratory disease There is provided a pharmaceutical composition for treating respiratory disease comprising an NO-donating steroid and at least one bronchodilator. Also provided is a method for treating respiratory diseases associated with inflammation comprising administering an NO- donating steroid with at least one bronchodilator. Use of the combination of an NO-donating steroid with at least one bronchodilator for treating respiratory disease is also provided.
CN103356649A Application of Chukrasone A in preparing anti-hypoxic medicines The invention discloses an application of Chukrasone A in preparing anti-hypoxic medicines. The anti-hypoxic effect of Chukrasone A is observed through integral and cellular level hypoxic models. Results show that Chukrasone A can remarkably improve the survival rate and the survival time of mice with chocking hypoxia and acute decompression hypoxia, alleviate myocardial damage of mice with drug specific hypoxia, and further has a remarkable protective effect to hypoxia injury of cardiac myocytes and nerve cells of neonatal rats cultured in vitro. The invention provides a use of Chukrasone A in preparing anti-hypoxic medicines.
US7473416 Medicaments for asthma treatment A method and apparatus are disclosed for treating asthma and other respiratory conditions. A medicament comprising a surface active phospholipid (SAPL) is prepared in the form of a fine powder and administered to the lungs in a gas stream. A preferred SAPL is a solid blend of diplamitoyl choline and phosphatdiyl glycerol (PG).
CN101434616B Organotin Schiff base coordination compound, as well as preparation method and application thereof The present invention discloses an organotin schiff alkali coordination compound, the structure thereof is shown as the formula, and a preparation method thereof comprises the following steps: 2.5mmol to 3.0mmol of 2-hydroxyl naphthaldehyde 1, 4-benzyldiacylhydrazones, 10mmol to 15mmol of sodium ethanol and 50mL to 100mL of methanol are added into a round-bottom flask and stirred for 0.5 hour to 2 hours; and then 2.5mmol to 5.0mmol of dibutyltin dichloride is added into the flask and heated up for reflux for 5 hours to 8 hours under the condition of stirring,; after that, the mixture is cooled and filtered and the filtrate is evaporated and dried by a rotary evaporator to obtain a yellow solid; the yellow solid is recrystallized by dichloromethane ethanol to obtain an orange crystal which is the organotin schiff alkali coordination compound. The organotin schiff alkali coordination compound has higher anticancer activity and can be applied as the raw material in the preparation of medicaments used for treating stomach cancer, nasopharyngeal cancer, liver cancer or leucocythemia. Compared with common-used platinum-based anticancer medicaments, the organotin schiff alkali coordination compound is characterized by high anticancer activity, good fat solubility, low cost, simple preparation method and the like and provides a new approach for developing anticancer medicaments.
WO2014099705A1 Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds The present invention relates to the compound of the formula or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
CN101904820A Quercetin nanosuspension freeze-drying composition and preparation method and application thereof The invention relates to a quercetin nanosuspension freeze-drying composition and a preparation method and application thereof. The composition comprises quercetin, a surfactant and a freeze-drying protectant and has grain size being less than 300nm after being re-dispersed in water. The injection which is prepared by the freeze-drying composition and can be used for intravenous injection does not need any organic solvent, thus reducing the irritation and improving the curative effect. The composition selects the auxiliary materials which are used for injection, thus being simple in composition, and the preparation method is economic and reliable and has industrial production prospect.
US20120329816 Methods for Altering MRNA Splicing and Treating Familial Dysautonomia and Other Mechanistically Related Disorders This invention relates to methods for altering the splicing of mRNA in cells. In particular, this invention also relates to methods for increasing the ratio of wild type to misspliced forms of mRNA and corresponding encoded proteins in cells possessing a mutant gene encoding either the i) misspliced mRNA corresponding to the mutant protein or ii) a component in the splicing machinery responsible for processing the misspliced mRNA. In addition, this invention relates to treating individuals having a disorder associated with a misspliced mRNA, such as Familial Dysautonomia or Neurofibromatosis 1, by administering to such an individual a cytokinin such as kinetin.
WO2008119657A1 Imidazolidinone derivatives The invention is concerned with novel imidazolidinone derivatives of formula (I) wherein R 1 to R 11 and X are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.
CN102068702A Lactosyl-norcantharidin phospholipid compound and preparation method thereof The invention discloses a lactosyl-norcantharidin phospholipid compound which is obtained by bonding hydrogen bonds with phospholipid and a large amount of -OH in lactosyl-norcantharidin. In the novel compound, the lipid solubility of the lactosyl-norcantharidin is improved while the original anti-cancer activity of the lactosyl-norcantharidin is kept, thus the absorption of the lactosyl-norcantharidin in human body can be improved and the bioavailability can be increased. The lactosyl-norcantharidin phospholipid compound is a novel compound which is obtained by connecting lactosyl-norcantharidin with the phospholipid through hydrogen bonds, and has better lipid solubility. The preparation method is simple, the yield is high, and the lactosyl-norcantharidin phospholipid compound has the functions of improving the in vivo absorption of medicament and improving the effect for treating liver caner on the basis of keeping the original antitumor function.
EP0833651B1 Analgesic use of n-l-alpha-aspartyl-l-phenylalanine 1-methyl ester N-L-α-aspertyl-L-phenylalanine 1-methyl ester and/or its derivatives has been found to have analgesic pain relieving properties in both humans and animals. It has been found to be especially effective in relieving pain associated with osteoarthritis and multiple sclerosis. It can be administered by itself or in combination with other analgesics. When given in combination with other analgesics, N-L-α-aspartyl-L-phenylalanine 1-methyl ester and/or its derivatives helps to alleviate the detrimental side effects of other analgesic medications by lowering the dosage requirements for pain relief.
CN102973925A Preparation method of composition for promoting wound healing The invention provides a preparation method of a composition for promoting wound healing. The preparation method comprises the following steps of: (1) dissolving 0.5 to 2.5 percent of chlorhexidine acetate and 1 to 3.5 percent of prednisolone acetate in 5 to 15 percent of sterile water; (2) adding 2 to 5 percent of dodecyl dimethyl benzyl ammonium chloride and 0.05 to 0.3 percent of vascular endothelial growth factor, and uniformly stirring; and (3) filling ointment base till 100 percent, and sufficiently and uniformly stirring to obtain a finished product. According to the composition prepared by the method, the time of wound healing can be remarkably shortened, and the scar width can be effectively reduced.
US20090061022 Pharmaceutical composition comprising arsenite for the treatment of malignancy A method for using sodium meta-arsenite (AsO2 −) to suppress growing of human cancer cells is provided to find a method of curing human cancers. Effects of sodium-meta arsenite (AsO2 −) on various human cancer cells are investigated via in vitro cytotoxic activity and in vivo anticancer activity against nude mice. For in vitro cytotoxic activity, six (6) kinds of human cancer with nine (9) cancer cell lines, eight (8) kinds of human cancers with twelve (12) cancer cell lines and ten (10) kinds of human cancers with forty one (41) cancer cell lines are tested. For in vivo anticancer activity, two (2) kinds of cancers of human renal cancer RXF 944LX and leukemia cells are tested utilizing nude mice. Maximum tolerated dose assessment of sodium meta-arsenite (AsO2 −) after daily oral gavages for 14 days were investigated for mouse, rat and pig. Subacute toxicity study of sodium meta-arsenite (AsO2 −) was induced after daily oral gavages for 14 days in the mouse followed by a 28-day recovery period. Arsenic acid sodium salt and cacodylic acid were used for comparison of the effect on the same human cancer cell lines. Sodium meta-arsenite (AsO2 −) showed better anticancer activity without any severe side effects within the range of tested dose compared to other arsenic compounds.
CN1943579A Use of asiatic acid in preparing medicine The new use of astatic acid in manufacturing drugs is disclosed, particularly the use in the aspect of manufacturing drugs for anti hepatic fibrosis.
WO2008002449A3 Glycomimetic inhibitors of siglec-8 Compounds, compositions and methods are provided for detecting or modulating in vitro and in vivo processes mediated by Siglec-8 binding. More specifically, Siglec-8 modulators and their use are described, wherein the Siglec-8 modulators that modulate a Siglec-8-mediated function comprise particular glycomimetics alone or linked to a diagnostic or therapeutic agent.
WO2007006544A3 Cyclic adenosine monophosphate compounds for the treatment of immune-related disorders The present invention is related to the finding that certain analogues of cAMP such as 8-(4-chlorophenylthio)- 2'- O- methyladenosine- 3', 5'- cyclic monophosphate (8-pCPT-2'-O-Me-cAMP) specifically blocks the production of IL-10 in human T cells. It is also related to the finding that the production of other cytokines (e.g. IL-2, IL-4, IL-5, IL-6, IL-12 and IFN-gamma) is not affected by these analogues. The finding may be used as a treatment of conditions which respond to a reduced level of IL-10 and/or by a change in the balance of the Th1 and Th2 responses. It may be used in research and in testing for dysfunctional EPAC protein and IL-10 producing pathways.
CN102000051A Application of 5-caffeoylquinic acid in preparing anti-tumor drugs The invention relates to an application of 5-caffeoylquinic acid in preparing anti-tumor drugs, belonging to the technical field of drug preparation. The invention also relates to an anti-tumor drug containing the 5-caffeoylquinic acid, which is prepared from the following components by weight percent: 0.05-99% of 5-caffeoylquinic acid and 1-99.5% of pharmaceutically acceptable carrier. The 5-caffeoylquinic acid has the effect of inhibiting angiogenesis and can inhibit the growth and transfer of tumors by inhibiting tumor angiogenesis, thus realizing the purpose of tumor resistance.
CN1615870A Itraconazole freeze-dried powder injection and preparing method The freeze-dried Itraconazole powder for injection is prepared through preparing solution with Itraconazole, hydroxypropyl-beta-cyclodextrin, propylene glycol, hydrochloric acid and sodium hydroxide; adding proper amount of diluent and freeze drying. Compared with Itraconazole injection, the present invention has the advantages of raised physical stability, no high temperature decomposing degradation of Itraconazole, loose product and fast recovering of the original solution characteristic after adding water, low water content and drying in vacuum resulting in less oxidation and high stability for long term storing, and less pollution and particle matter introduced during production.
CN101897751B Application of pharynx-clearing dropping pills in preparing antiviral drugs The invention discloses an application of pharynx-clearing dropping pills in preparing antiviral drugs. The experiment proves that the pharynx-clearing dropping pills act with herpes simplex viruses and adenovirus in vitro under the temperature of 37 DEG C for one hour, viruses can be effectively inactivated and infectivity of the viruses can be lost; and the pharynx-clearing dropping pills play roles of obviously inhibiting and blocking herpes simplex viruses and adenoviruses from invading the cells in the in-vitro cellular level, with a certain dose-response relationship; and in the in-vivoexperimental research, the mortality rate of mice which utilize the pharynx-clearing dropping pills to cure the infected influenza viruses indistinctively differs from that of a model group, however,survival days of the mice can be obviously prolonged and morbidity thereof can be delayed. The fact is found by detecting all immune indicators of the mice that the pharynx-clearing dropping pills can mobilize immunity after the mice are infected with influenza virus to a certain extent. Therefore, the pharynx-clearing dropping pills have a certain effect on mouse with anti-influenza virus FM1 strain and regulation of organism immunity; and in addition, the pharynx-clearing dropping pills can inhibit coxsackie virus B3.
US20080193574 Central nervous system disorders;Alzheimer's disease; using ginger oil Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and Alzheimer's disease with a derivative of ginger oil are also provided. Also provided is a method of conditioning biological extracts, such as a medicinal plant extract, by a reductive amination process to give nitrogen-containing derivatives.
US20110091511 Transdermal delivery of drugs based on crystal size A blend of at least two polymers in combination with a drug provides a pressure-sensitive adhesive composition for a transdermal drug delivery system in which the drug is delivered from the pressure-sensitive adhesive composition and through dermis when the pressure-sensitive adhesive composition is in contact with human skin. According to the invention, providing drug having differing crystal sizes as well as drug which is solublized in the pressure-sensitive adhesive composition controls the rate of drug delivery from the pressure-sensitive adhesive composition.
CN1721413A Barbituric acids and their preparation process and use The present invention relates to one new kind of barbituric acid compound and its application as protein tyrosine phosphatase inhibitor in preventing and treating diabetes and its preparation process.
CN101069746B Composition containing sugar-reducing medicine and antiplatelet medicine The present invention relates to a medicine composition containing hypoglycemic medicine (mainly including thiazolidione, biquanide or alpha-glycosidase inhibitor) and antiplatelet medicine (mainly including aspirin or clopidogrel). Said medicine composition contains hypoglycemic medicine or its medicinal salt with effective dose and medicinal carrier or excipient. Said invention also provides the application of said medicine composition in preparation of medicine for curing the diseases of hypertension, diabetes, inflammation and atherosclerosis, etc.
CN103690582A Composition containing dendrobium polysaccharide and atractylodes oil and application thereof The invention provides a composition containing dendrobium polysaccharide and atractylodes oil and application thereof. The composition contains dendrobium polysaccharide, atractylodes oil and pharmaceutically acceptable auxiliaries for treating or preventing effective dose, and can be applied to preparation of medicines or health-care foods for preventing or relieving gastric ulcer.
WO2007016679A3 Combination immediate release controlled release levodopa and carbidopa dosage forms The present invention relates to pharmaceutical dosage forms of a combination of carbidopa and levodopa comprising both immediate release and controlled release components for the treatment of ailments associated with depleted amounts of dopamine in a patient's brain tissue, which dosage forms display no food effect or at least substantially avoid the food effect, and a related method of treatment for a patient in which the bioavailability of levodopa under non-fasting conditions is equivalent to the bioavailability under fasting conditions.
US20100178251 Dual-Sensitizer-Containing Luminescent Compounds, Conjugates, and Uses Thereof The invention relates to novel luminescent compositions of matter containing two fluorophores (sensitizers), synthetic methods for making the compositions, macromolecular conjugates of the compositions, and the use of the compositions and their conjugates in various methods of detection. The invention also provides kits containing the compositions and their conjugates for use in the methods of detection.
WO2012115177A1 N-[(biaryloxy)alkylcarbonyl]sulfonamide derivative The present invention provides a compound which has excellent anti-platelet aggregation activity and is useful for prophylaxis and/or treatment of thromboembolic diseases. A compound represented by general formula (I) or a pharmacologically acceptable salt thereof. (In general formula (I), n represents 1 or 2; R1 represents a halogen atom, a cyano group, an amino group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group; R2 represents a hydrogen atom, a halogen atom, a cyano group or a C1-4 alkyl group; R3 and R4 each represents a hydrogen atom, a C1-4 alkyl group, a halogenated C1-4 alkyl group, a C1-4 alkoxy C1-4 alkyl group or a group that forms a C3-5 cycloalkyl group; R5 represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, a C1-4 alkyl group or an amino group; R6 represents a hydrogen atom, a halogen atom or a C1-4 alkyl group; R7 and R8 each represents a hydrogen atom, a halogen atom or a C1-4 alkyl group; R9 and R10 each represents a hydrogen atom or a C1-4 alkyl group; R11 represents a C1-4 alkyl group or a phenyl group; X represents an oxygen atom, a sulfur atom or -CH2-; Y represents a nitrogen atom or =C(Ra)-; Ra represents a hydrogen atom, a halogen atom or a C1-4 alkyl group; and Z represents a nitrogen atom or =CH-.)
WO2010033598A2 System and method for utilizing microbubbles and liposomes as viral sequestering agents A system and method of utilizing microbubbles and liposomes as viral sequestering agents. Microbubbles and liposomes having polyanions and conjugation systems are injected into the bloodstream of a subject human or animal. The microbubbles and/or liposomes attract virus particles including envelope viruses. After the microbubbles and/or liposomes have circulated in the blood for a pre-established time period, the microbubbles and/or liposomes along with attached virus particles are separated from the blood of the subject by passing the blood over or through a substrate or using a centrifuge. The substrate includes a conjugation system which has an affinity for the polyanions of the microbubbles and/or liposomes. As the microbubbles and/or liposomes and attached virus particles are removed from the blood, the viral titer of the subject is lowered. The microbubbles and/or liposomes may also be mixed with blood and filtered outside of the subject such that the microbubbles and/or liposomes are never in the bloodstream of the subject.
CN102525981A Propranolol hydrochloride tablets and preparation method thereof The invention relates to a preparation method for propranolol hydrochloride tablets. The method comprises the following steps of: 1) preparing a carrier for solid dispersoid, namely weighing 200 grams of polyethylene glycol (PEG) 6000, dissolving the PEG 6000 in 95 percent (ml/ml) ethanol to obtain an auxiliary material solution, dissolving 100 grams of propranolol hydrochloride in 95 percent (ml/ml) ethanol to obtain a main medicine solution, mixing the auxiliary material solution and the main medicine solution uniformly to obtain a mixed solution, and drying the mixed solution at temperature of between 35 and 55 DEG C under the vacuum with the vacuum degree of less than 10 Pa for 12 to 24 hours; 2) preparing tablets, namely crushing the materials obtained in the step 1), and sieving to obtain solid dispersoid powder; adding a formula dose of dextrin into the solid dispersoid powder, and putting the mixture into a granulator, performing dry mixing for 5 to 10 minutes, adding 40 to 50 percent ethanol serving as an adhesive, and granulating; sieving the materials with a 20-to-30-mesh sieve, granulating in the wet state, and transferring to a fluidized drying machine for drying until the moisture is 5 to 8 percent; and sieving the dried granules with a 20-to-30-mesh sieve, granulating, and mixing the obtained granules and a lubricating agent in a formula uniformly for tabletting.
CN102573828A Cell protection in dialysis patients by administration of a creatine compound The invention relates to a dialysis solution for haemodialysis or peritoneal dialysis, said solution having a theoretical osmolarity within the range of from 250 to 550 mosm/L and a pH value within the range of from 4.9 to 8.0, said solution comprising a creatine compound and one or more electrolytes, wherein the concentration of the creatine compound is not more than 50 mM
US20080015195 Novel Heteroaromatic Inhibitors of Fructose-1,6-Bisphosphatase Novel FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
CN103301453A Freeze-dried vaccine for porcine reproductive and respiratory syndrome and preparation method thereof The invention relates to a freeze-dried vaccine for porcine reproductive and respiratory syndrome and a preparation method thereof. The freeze-dried vaccine is prepared from a porcine reproductive and respiratory syndrome viral antigen and a protective agent, wherein the protective agent is prepared from the following substances by weight percent: 2-3% of NZ-Amine AS, 0.1-0.3% of glutamic acid mono potassium salt, 10-15% of cane sugar, 1-2% of lactoalbumin hydrolysate, 10-20% of hydrolyzed gelatin, 0.1-0.2% of vitamin C and the balance of water for injection. The heat-resisting protective agent is capable of minimizing injuries caused by various physical and chemical factors to virus activity during processes of sub-packaging and freeze-drying products, so that the titer loss of a virus before and after freeze-drying is reduced to be not more than 0.2 titer; and the live vaccine of the heat-resisting protective agent is high in anti-aging degree, the loss ratio of the virus does not exceed 0.5 titer after the vaccine is preserved for 10 days at the temperature of 37 DEG C, the titer reduction of the vaccine is little after the vaccine is preserved for 24 months at the temperature of 2-8 DEG C, and therefore, the problems of energy waste and preservation inconvenience caused by a strict cold chain condition required in transportation and preservation of conventional vaccines are effectively solved.
US20120121665 Implantable or insertable medical device resistant to microbial growth and biofilm formation Disclosed are implantable or insertable medical devices that provide resistance to microbial growth on and in the environment of the device and resistance to microbial adhesion and biofilm formation on the device. In particular, the invention discloses implantable or insertable medical devices that comprise at least one biocompatible matrix polymer region, an antimicrobial agent for providing resistance to microbial growth and a microbial adhesion/biofilm synthesis inhibitor for inhibiting the attachment of microbes and the synthesis and accumulation of biofilm on the surface of the medical device. Also disclosed are methods of manufacturing such devices under conditions that substantially prevent preferential partitioning of any of said bioactive agents to a surface of the biocompatible matrix polymer and substantially prevent chemical modification of said bioactive agents
CN101264121B Blood fat reducing health products and preparation The invention relates to a health care product reducing blood fat and the preparation method, which is characterized in that: the health care product uses Chinese radish seed, epimedium brevicornum, American ginseng, ganoderma lucid extraction, Vitamin E, beta-carotene as main raw material. The health care product reducing blood fat has the advantages of lowering concentration of triglyceride in blood fat of small mice, lowering lipid peroxide, cleaning free radical and anti-peroxidation, having certain improvement upon fatty liver, lowering triglyceride without toxicity through animal experiment showing.
US7144865 Daily administering a mixture of zinc salt, cyclo-Hispro (soybean protein product), arachidonic acid; treating hypertension, high cholesterol, weight control; nutritional supplements, foods The present invention relates to dietary supplementing methods useful for controlling obesity. More particularly, the invention relates to methods of administration of compositions containing defined chemical species useful for prevention and treatment of obesity. In a preferred embodiment, pharmaceutical compositions used in connection with the present invention comprise: (1) a zinc salt, (2) cyclo-Hispro and/or (3) arachidonic acid, and (4) at least one pharmaceutically acceptable excipient. More particularly, the invention relates to methods of manufacturing of preparing a soybean protein hydrolysate (SPH) comprising cyclo-Hispro.
US7569696 Process for producing crystal The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.n′H2O (wherein n′ is about 0 to about 0.1) or a salt thereof, which characteristically includes crystallization from an organic solvent solution or suspension in which (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-benzimidazole.nH2O (wherein n is about 0.1 to about 1.0) or a salt thereof has been dissolved or suspended, and the like, and provides a convenient method for efficiently producing an optically active sulfoxide derivative having an extremely high enantiomer excess in high yield at an industrial large scale.
US7223755 Such as (2S,5S)-5-benzyl-6-hydroxy-2-(2-methylpropyl)-3-morpholinone, which has calpain inhibitory activity; for treating cataract or retinal ischemic disorder A compound represented by the following formula (I) wherein R1 and R2 are each a lower alkyl group optionally having substituents, which has a calpain inhibitory activity, or a salt thereof is provided.
WO2005111213A1 Target gene mimitin of myc Novel diagnosis and treatment for cancer. There are provided target protein Mimitin of cancer gene myc protein, its variant, fragments thereof, and polynucleotide molecules coding for them. A substance capable of inhibiting any biological action by binding between a polynucleotide molecule coding for Mimitin protein and Myc provides useful means for the diagnosis, prevention or treatment of cancer.
US20090246170 Therapeutic Agent For Alzheimer's Disease The present invention provides novel therapeutic methods and agents for treating Alzheimer's disease. Specifically, the present invention relates to anti-inflammatory cytokines, anti-inflammatory cytokine genes, negative-strand RNA viral vectors carrying an anti-inflammatory cytokine gene, which are used for treating Alzheimer's disease or developing therapeutic agents for Alzheimer's disease. The present invention also provides pharmaceutical compositions for treating or preventing Alzheimer's disease, which comprise the cytokines or vectors. The present invention further provides methods for treating Alzheimer's disease, which comprise the step of administering an anti-inflammatory cytokine, or a vector such as a negative-strand RNA viral vector carrying an anti-inflammatory cytokine gene. The present invention enables novel gene therapies for Alzheimer's disease.
CN102860986A Stable taste-masking levocetirizine medicine composition and preparation method thereof The invention provides a stable taste-masking levocetirizine medicine composition and a preparation method thereof. The medicine composition comprises levocetirizine, a taste masking agent and a stabilizer, the levocetirizine is levocetirizine hydrochloride, the taste masking agent is beta-cyclodextrin or a derivative thereof, and the stabilizer is sodium citrate. Other pharmaceutically acceptable auxiliary materials are selectively added in the medicine composition, the medicine composition can be further prepared into granules, orally disintegrating tablets and chewable tablets, tastes good, is quick in absorption, stable in quality, simple and feasible in preparation process, and can be produced in batches by using the conventional pharmaceutical equipment, and the related medicinal auxiliary materials are easy to purchase and low in cost.
WO2007128725A1 6h-benzofuro[3,2-c] [1]benzopyran and [2] benzopyrano [4,3-b] [1]benzopyran derivatives and wood extracts of these compounds as aryl hydrocarbon receptor (ahr) antagonists for the prevention of uv-b induced skin damage The invention relates to the field of aryl hydrocarbon receptor (Ah receptor; AhR) antagonists and to a compound of formula (lII) or (V) in which R1 to R10 independently of one another can be hydrogen, hydroxyl, C1-C10-alkyl, C1-C10-alkenyl, C1-C10-alkoxy, prenyl or O-glycosyl, and two radicals R1 to R10 can be joined via a methylenedioxy group -O-CH2-O-, and R5 can be replaced by a double bond, as a drug, which is intended for (a) reducing or preventing a translocation of the AhR into a cell nucleus, (b) reducing or preventing a UVB-induced or UVB-inducible gene expression, (c) reducing or preventing a gene expression induced or inducible by polycyclic aromatic hydrocarbons, preferably TCDD, and/or (d) reducing or preventing UVB-induced or UVB-inducible skin damage, especially skin cancer, skin ageing, skin inflammations and sunburn; as well as to process for the preparation of a drug, comprising the extraction of wood.
WO2012064301A3 Physically improved tablet formulations The present invention relates to physically improved tablet formulations of a leukotriene receptor antagonist and combinations of the leukotriene receptor antagonist with an H1- antihistaminic which are effective in prevention and/or treatment of allergic and inflammatory diseases of the skin or upper and lower respiratory tracts and relieving the symptoms thereof.
US20080280957 Heterocyclic Inhibitors of Mek and Methods of Use Thereof Disclosed are MEK inhibitors useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
EP1553937B1 Glycinenitrile-based inhibitors of dipeptidyl peptidase iv A compound of the Formula (I) wherein R1, R2, R3 and R4 are as defined herein. Further provided are methods of using such compounds for the treatment of diabetes and related diseases, and to pharmaceutical compositions containing such compounds.
US20120177733 Solid dosage forms of valsartan and amlodipine and method of making the same Monolayer and bilayer solid dosage forms of a combination of valsartan and amlodipine are made.
US20090326059 Benzyloxy anilide derivatives useful as potassium channel modulators The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
CN102138993A Hyperosteogeny ointment The invention discloses hyperosteogeny ointment which is an external ointment medicament for treating hyperosteogeny of joints, composes of borneol, long-noded pit viper, cinnamon, dandelion, rhubarb, fructus gardeniae, pawpaw, ground beetle, frankincense, musk, hony and vaseline. All the medicinal materials have synergistic actions to play the efficacies of promoting the restoration of consciousness, dispersing stagnated fire, promoting the subsidence of swelling, alleviating pain, clearing away heat and toxic material, promoting urination, reducing the stagnation, expelling wind-damp, penetrating bones and muscles, removing obstruction in channels, dissipating blood stasis and the like. The hyperosteogeny ointment has notable curative effects, quick effect taking speed and high cure rate in treating hyperosteogeny of joints, has the effects on treating both principal and secondary aspects of disease, and can achieve the aim that hyperosteogeny is not liable to relapse after healing.
EP2347757A1 A natural allicin tablet and preparation method thereof A natural allicin tablet and preparation method thereof are provided in the invention, wherein the allicin tablet has a high allicin content per gram tablet weight. The allicin tablet exhibits a better effect in antibacterial, antiphlogistic and antivirus and it is safe to human drug-administration.
CN101229141B Aspirin sustained release tablet and preparing method thereof The invention relates to the field of pharmaceutical preparation, in particular to a sustained-release aspirin tablet, and is characterized by consisting of aspirin with 75 portions, ethyl cellulose with 10 to 25 portions, polyacrylic resin with 7.5 to 10 portions, starch with 4 to 10 portions, hydroxypropyl methyl cellulose with 1 to 6 portions, tartaric acid with 0.32 to 0.64 portions, talcum powder with 2.7 to 3.6 portions. The invention also discloses a pharmaceutical preparation method.
WO2010019276A2 Method and formulation for treating adverse biological conditions A method for treatment of adverse biological conditions is provided, wherein a biologically active agent such as a macromolecular biomolecule, e.g., a nucleic acid or a peptidic compound, is administered to a subject in need of such treatment in a formulation containing a transport enhancer having the structure of formula (I) wherein Q, R1, and R2 are as defined herein. Methylsulfonylmethane (MSM) is a representative and preferred transport enhancer. Formulations are also provided.
CN103127072A Application of Eryngiolide A in medicines curing yellow fever virus infection The invention discloses application of Eryngiolide A in preparation of medicines curing or preventing yellow fever virus infection. The Eryngiolide A can effectively inhibit proliferation of the yellow fever virus, but has small toxicity to cells, can be further developed into medicines curing disease caused by the yellow fever virus, and has broad application prospect. Use of the Eryngiolide A in preparation of medicines curing the Alzheimer disease is made public for the first time, the skeleton type is completely novel, and the Eryngiolide A has an unexpectedly high yellow fever virus inhibitory activity, probability of other compounds giving any revelation for the Eryngiolide A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in preventing and curing the yellow fever virus infection.
WO2006116953A1 A method for the preparation of tegaserod and slected salts thereof A method of preparing tegaserod of formula (I) and pharmaceutically acceptable salts derived therefrom.
WO2005023766A1 Salt of atorvastatin with metformin A novel compound of formula (I), a mutual salt of atorvastatin and metformin, is disclosed. The compound of formula (I) can be used for the treatment of hyperlipidemia and hyperglycemia.
WO2011149995A1 Novel substituted octahydrocyclopenta [c]pyrrol-4-amines as calcium channel blockers The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
US7875605 1-Benzenesulfonyl-3-(4-methylpiperazin-1-ylmethyl)-5-nitro-1 H-indole; 1-[[5-Bromo-1-(2-Bromo-4-methoxybenzenesulfonyl)-indo1-3-yl]methyl][1,4]diazepane; useful for treating psychotic and neurodegenerative disorders e.g. schizophrenia, Alzheimer's disease, Parkinson's disease and Huntington's chorea N-arylsulfonyl-3-substituted indole compounds, derivatives, analogs, tautomeric forms, stereoisomers, geometric forms, N-oxides, polymorphs and pharmaceutically acceptable salts.
US20060252810 e.g. 5-(4-Fluorophenyl)-4-(4-pyridinyl)imidazole-2-thio-3-propyl-N-phthalimide; immunomodulating and cytokine-release-inhibiting action; antiinflammatory agent The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3, R4 and p are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.
CA2405429C Minoxidil-containing preparation The present invention provides a minoxidil-containing composition which can be prevented from coloring for a long period of time. The composition, which comprises an anti--oxidant such as dibutyihydroxytoluene, butylhydroxyanisole or erythorbic acid, and has a pH of from 5.5 to 7Ø
EP1562577B1 Acetyl-l-carnitine for the prevention and/or treatment of peripheral neuropathies induced by thalidomide This invention disclosed the use of acetyl L-carnitine or of a pharmaceutically acceptable salt thereof for the preparation of a medicament for preventing and/or treating peripheral neuropathies induced by the administration of a peripheral neuropathy-inducing anticancer agent. In particular said anticancer agent is selected from the group consisting of the family of platin compounds, taxanes, epothilone class and vinca alkaloids, farnesyl transferase inhibitors, thalidomide, 5-fluorouracil, cryptophycin analogues, proteasome inhibitors. Said medicament can be administered in a co-ordinated manner to a subject suffering from said peripheral neuropathies, or expected to suffer from said peripheral neuropathies. Beneficial effects on the patient’s quality of life are achieved and an improvement of therapeutic index of the anticancer agent is obtained.
US20110189141 Multiple target t cell receptor The present invention is directed to a functional T cell receptor (TCR) fusion protein (TFP) recognizing and binding to at least one MHC-presented epitope, and containing at least one amino acid sequence recognizing and binding an antigen. The present invention is further directed to an isolated nucleic acid molecule encoding the same, a T cell expressing said TFP, and a pharmaceutical composition for use in the treatment of diseases involving malignant cells expressing said tumor-associated antigen.
US20080081780 Identification of oligoadenylate synthetase-like genes The present invention relates to compositions and methods for modulating conception in animals. More particularly, the composition modulates mRNA degradation during gametogenesis and early development. Yet further, the present invention relates to pharmaceutical compositions and methods for modulating diseases of the reproductive organs, such as hyperproliferative diseases.
CN1683381A Trifolium pratense extract and preparing method The present invention relates to red clover extract and its preparation process. The red clover extract is obtained with red clover herb as material and through alcohol extraction and purification and detected in HPLC process. The extract has isoflavone amount not less than 12.0 % accounting in formononetin and sophoricol. The present invention also discloses the quality control method of red clover herb. The present invention has simple extracting process and perfect quality control, can ensure accurate dosage and reliable curative effect, and is suitable for industrial production.
CN1938429A Oligosaccharides, preparation method and use thereof, and pharmaceutical compositions containing same The invention relates to oligosaccharides, the preparation method and use thereof, and pharmaceutical compositions containing same. More specifically, the invention relates to oligosaccharides which can be used for the treatment of cancer and, in particular, to prevent and inhibit the formation of metastases. The inventive oligosaccharides can be used, for example, during early breast, lung, prostate, colon or pancreatic cancer. The oligosaccharides can be administered subcutaneously, orally or intravenously. Moreover, said oligosaccharides can be used alone or together with other anticancer agents, e.g. cytotoxics such as docetaxel or paclitaxel.
WO2007043363A1 Composition for use in prevention of hypoglycemic condition Disclosed is a composition for use in the prevention of a hypoglycemic condition, which comprises at least one compound selected from a branched amino acid, a pharmaceutically acceptable salt thereof and a derivative of the amino acid or salt as an active ingredient. The composition can promote the uptake of a saccharide into a brain cell to thereby prevent a hypoglycemic condition.
CN103735538A Medical application of radix arnebiae seu lithospermi naphthoquinone compounds The invention discloses application of radix arnebiae seu lithospermi naphthoquinone compounds to preparation of medicaments for treating Crohn's disease. The invention further discloses medical application of one or more radix arnebiae seu lithospermi extracts with a formula shown in the specification.
US6864262 Bladder disorders; incontinence; side effect reduction The present invention provides a compound of the formula (I) and the pharmaceutically acceptable salts and solvates thereof, which is useful for treating bladder over-activity or urinary incontinence.
WO2010110923A2 Prophylactic and therapeutic treatment of alzheimer's disease A composition and method for the treatment of Alzheimer's disease and related amyloid plaque development and reduction of amyloid plaque, amyloidosis and amyotrophic lateral sclerosis, includes an effective amount of a compound selected from the group consisting of phytic acid, a phytate salt, an isomer or hydrolysate of phytic acid or a phytate salt, or a mixture of any combination thereof, being administered to a person in an amount from about 0.5 grams to about 18.75 grams per day.
CN102188493B Compound Yinqiao Anmin capsule The invention belongs to the technical field of pharmacy, and in particular provides a novel compound Yinqiao Anmin capsule. The capsule contains acetaminophen, chlorphenamine maleate, vitamin C, lonicera and forsythia extract, peppermint oil, fructus forsythiae volatile oil, schizonepeta volatile oil and cyclodextrin. The volatile oil components in the compound Yinqiao Anmin capsule provided by the invention are stable for a long time, thus ensuring the accuracy of the preparation formula and the curative effects of the capsule.
US20120238596 Formulations comprising palonosetron Pharmaceutical compositions comprising palonosetron and its pharmaceutically acceptable salts, in the form of a ready-to-use solution or a lyophilized form. Specific embodiments of the invention relate to stable pharmaceutical formulations of palonosetron and its pharmaceutically acceptable salts, wherein the formulation does not comprise a chelating agent or an antioxidant.
CN101890045A External medicament for treating infantile eczema The invention discloses an external medicament for treating infantile eczema, which is characterized by comprising the following ingredients in percentage by weight: 23.75 to 26.25 percent of zinc oxide, 23.75 to 26.25 percent of starch, 0.24 to 0.26 percent of furacilin, 1.90 to 2.10 percent of miconazole nitrate, and 45.36 to 50.14 percent of vaseline. The external medicament has the advantages of simple ingredients, convenient operation, small side effect and high curative rate, and is particularly applicable for treating infantile eczema.
CN102048708A Tinidazole vaginal effervescent tablet and preparation method thereof The invention relates to a tinidazole vaginal effervescent tablet and a preparation method thereof. The tinidazole vaginal effervescent tablet has the advantages of simple preparation method, good treatment effect and the like. The tinidazole vaginal effervescent tablet comprises the following components in parts by weight: 200 parts of tinidazole, 105 parts of tartaric acid, 40 parts of calcium lactate, 44 parts of lactic acid, 150 parts of starch, 6.5 parts of polyvidone K30, 20 parts of silicon dioxide, 120 parts of sodium bicarbonate, 60 parts of polyethylene glycol 4000, 4 parts of lauryl sodium sulfate and 4 parts of magnesium stearate.
EP2116538A1 Condensed tetrahydroquinoline derivative and use thereof for medical purposes The problem of the present invention is to provide a compound having a GR selective binding activity, which shows less action on other nuclear receptors such as progesterone receptor (PR), mineralocorticoid receptor (MR) and the like. The present invention provides a condensed tetrahydroquinoline compound represented by the following formula (I) wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof or a hydrate thereof.
CN1634070A Eye drop of pazufloxacin mesilate, its preparing method and application The disclosed eye drop is prepared from Pazufloxacin mesilate, preservative agent, stabilizer, viscosity increaser and solvent through the steps of, (1) preparing boric acid and cushion liquid, (2) charging preservative into buffer agent, heating, stirring, dissolving and charging into stabilizing agent, charging Pazufloxacin mesilate, heating and stirring till dissolving, obtaining solution 1, (3) charging viscosity increaser into buffer agent or boric acid water, stirring till dissolving to obtain solution 2, (4) filtering the solution to obtained filtration liquid, (5) filtering the solution 2 to obtain filtration liquid, (6) merging the filtration liquid obtained in step (4) and (5), stirring, dissolving and charging into boric acid water or cushion agent, adjusting pH with hydrochloric acid or NaOH.
WO2005077462A3 Cd70 inhibition for the treatment and prevention of inflammatory bowel disease Substantially purified populations of APCLP cells capable of expressing CD70 are described. Also described are methods for the treatment of certain diseases and medical conditions of the gastrointestinal tract, such as inflammatory bowel disease, by utilizing inhibitors of CD70 activity.
CA2581658A1 Dibenzodiazepinone analogues, processes for their production and their use as pharmaceuticals The invention relates to biologically active dibenzodiazepinone analogues represented by Formula (I) where R1 is a linear C1-10 alkyl and the farnesyl moiety can have one, two or three hydrogenated or hydroalkoxylated double bonds), or a pharmaceutically acceptable salt or prodrug thereof, to pharmaceutical compositions comprising these compounds, methods of producing them, and their use in the preparation of medicaments for the treatment of neoplastic conditions.
WO2013066944A3 Biomarkers for cancer characterization and treatment Composition and methods for characterizing cancer cells by determining a marker of PKM2 activity. For example, methods are provided for predicting a patient response to a NF- κB, PKCε, PKM2, MEK/ERK, Pinl or Src inhibitor therapy. Methods for treating patients with such therapies are likewise provided. Phosphorylation selective β-catenin, MLC2, histone H3, Bub3, and PKM2 -binding antibodies are also provided.
CN102942562A Benzimidazole derivative, and preparation method and application thereof The invention relates to a benzimidazole derivative 2-m-phenylaminobenzimidazolyl-1H-pyrazolyl-3-formamide of which the structural formula is disclosed in the specification. The benzimidazole derivative can promote growth of microzyme, enhance the metabolic activity of the microzyme, obviously lower the plasma triglyceride, total cholesterol and high density lipoprotein of a C57 BL/6J mouse which is fed by high-fat feed for a long time, lower the contractive pressure and diastolic pressure of the model mouse, lower the fasting blood-glucose of the model mouse, improve the sugar tolerance of the mouse, influence the expression of SIRT1 and related genes (FOXO1, P53, PPARgamma and PGC-1alpha), and obviously improve the metabolism of glucose and fat; and therefore, the benzimidazole derivative can be used for preparing medicines for preventing and treating diabetes and complications thereof.
CN1602856A Calcium L-Threonate and soy bean isoflavone containing combination The invention relates to a combination containing L-and isoflavones of soybean and willing vitamin D3 for preventing or curing osteoarthritis, necrobiosis of caput femoris, osteoporosis or fracture, especially fracture caused by osteoporosis or for increasing one density, the weight ratio of L-and isoflavones of soybean is 1-1500:1-100. Experiment has proved that:(1).it can simulate cartilage cell to grow, so that promote growth and rapid of cartilage;(2) research result of rat osteoarthritis model has shown that the hurt to join cartilage can be reduced and can be prevented cured;(3). Inhibit bone absorption effect of the injured bone cell, stimulate growth of osteoblast cell and decrease synthesis of I-typed ossein;(4).help neogenesis and proliferation of bone blood vessel and advance bone blood cycling ;(5) increase bone density, calcification level and tenacity of bone, stress of strength of bone and energy for apply work;(6). It also has remarkable curative effect for curing necrobiosis of caput femoris.
CN1729993A Externally applied bath liquid for epidemic wind-heat type cold The invention provides a bath lotion for external use capable of treating common cold, which is prepared from (by weight ratio) Ribavirin solution 10-15%, dodecyl diethanol amine 8-12%, dodecayl triethanol amine sulfate 5-10%, sodium laureth sulfate 5-10%, and extract of natural plants including honeysuckle flower, capsule of weeping forsythia, Schizonepeta tenuifolia, mentha, arctium fruit, prepared soybean, root of ballon flower, mulberry leaf, wild chrysanthemum flower, peucedanum root, apricot seeds, isatic root, cordate houttuynia, hierochloe odorata, loquat leaves and licorice root.
WO2010053974A3 Stable organic peroxide compositons Benzoyl peroxide compositions containing antioxidants and/or malonic acid. Treatment of acne vulgaris with a combination of actives, namely benzoyl peroxide and salicylic acid, include applying such benzoyl peroxide compositions to an area of the body afflicted with acne followed by application of a topical, at least partially neutralized salicylic acid composition to the afflicted area. Malonic acid may be included in combination with either the benzoyl peroxide composition, the salicylic acid composition or both.
CN103168995A Health-care food for preventing diabetics The invention discloses a health-care food for preventing diabetics. The health-care food is characterized by comprising the following components: 25-40 parts of ginseng, 8-16 parts of tuckahoe, 8-16 parts of medlar, 21-30 parts of radix puerariae, 19-35 parts of coptis roots, 12-23 parts of Chinese yam, 10-15 parts of rehmannia roots, 5-19 parts of dogwood, 7-52 parts of semen cassiae, 3-10 parts of semen coicis, 10-30 parts of buckwheat husk flour, 70-100 parts of pumpkin, 5-40 parts of bee propolis and 5-15 parts of ganoderma lucidum polysaccharides. The health-care food has a two-way regulating effect for the blood sugar of a patient, can help a diabetic patient maintain the relative stability of the blood sugar, can also reduce the hunger sensation and is beneficial to weight loss and blood fat reduction. Pancreas cells are protected and recuperated so that a healthcare effect is achieved.
CN1887256A AIDS treating kadeli'an amine injection and freeze dried powder for injection and their prepn The present invention relates to injection, and is especially one kind of AIDS treating Kadelian amine injection and freeze dried powder for injection as retrovirus resisting medicine with obvious AIDS treating effect. The AIDS treating Kadelian amine injection and freeze dried powder for injection are prepared through dissolving methyl cantharidimide in compound solvent by means of solubilizing and subsequent conventional injection preparing steps. The present invention has direct and fast acting, less side effect, high safety and reliability and low cost.
WO2006097043A1 Bacopa monnieri extract and process for preparation and use thereof The present invention provides Bacopa monnieri extract, wherein total saponin of B. monnieri comprising 10% to 80% by weight of the extract, in terms of bacoside A. The present invention also provides pharmaceutical compositions comprising B. monnieri extract and process for preparation and use thereof. The present B. monnieri extract of various amount of bacoside A present is useful in various indications, with extensive clinical usage, reduced cost, enhanced controllability, and stable quality.
WO2005035507A3 4-aminopyrimidine derivatives for treatment of hyperproliferative disorders Pyrimidine derivatives of formula (I) in which J and Y represent aromatic or heteroaromatic rings; R2, G, G', and G' represent substituent groups and R2a represents H or halogen; L represents a linking group; and M represents CH or N. Pharmaceutical compositions containing these compounds, and methods of using these compounds in treatment of hyperproliferative diseases such as cancer are also disclosed and claimed.
US20110166171 Sustained release monoeximic formulations of opioid and nonopioid analgesics The present invention relates to monoeximic solid dosage forms for administering pharmaceutical agents, particularly Hydrocodone and acetaminophen, methods for preparing said dosage forms, and methods for providing therapeutic agents to patients in need of treatment.
CN101519385A Small molecule compound being capable of promoting proliferation of stem cells and function thereof The invention provides a small molecule compound capable of accelerating proliferation of stem cells and a function thereof. The compound plays an important role in the research of stem cell proliferation mechanism. The invention further relates to the function of the compound and relevant compounds thereof in the preparation of stem cell proliferation accelerators and the preparation of medicines accelerating stem cell proliferation. The invention also relates to the function of the compound in the preparation of medicines for treating various diseases arising from stem cell trauma. The diseases arising from stem cell trauma comprise diseases related to the retrogression or traumatism of nervous system cells, blood system diseases, diseases related to the loss or traumatism of cardiovascular system cells, skin burn and the like.
US20100041749 Organo-Arsenoxide Compounds and Use Thereof The present invention relates to organo-arsenoxide compounds and to methods for their synthesis. The invention also relates to pharmaceutical compositions comprising these compounds and to their use in the treatment of diseases and disorders, in particular proliferative diseases and disorders, including treatment of solid tumors and leukaemia.
WO2011101374A1 Compositions comprising amphetamin and lisdexamfetamine A formulation comprising dexamphetamine and lys-dexamphetamine useful in the treatment of ADHD or fatigue.
CA2685534A1 Use of matrix metalloproteinase inhibitors in skin care The application of matrix metalloproteinase (MMP) inhibitors to the skin inhibits the degradation of proteins found in the skin including collagen, elastin, and other basement membrane and extracellular matrix protein. MMP inhibitors may be used in both cosmetic compositions and pharmaceutical compositions for application to skin. MMP inhibitors are formulated with a cosmetically suitable vehicle or pharmaceutically acceptable excipient for application to the skin as creams, lotions, ointments, solutions, face masks, etc. As cosmetics, the inventive MMP inhibitor compositions are applied to the skin to prevent or reduce the appearance of wrinkles, pigmentation changes, loss of elasticity, or other effects associated with aging or sun damage. As pharmaceuticals, the inventive MMP inhibitor compositions may also be applied to the skin to treat or prevent a skin disease (e.g., proliferative disease, inflammatory disease).
WO2006024667A1 Furamate of 4-( (4-( (4- (2-cyanoethenyl) -2,6-dimethylphenyl)amino)-2-pyrimidinyl)amino)benzonitrile The present invention relates to the fumarate salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile, pharmaceutical compositions comprising as active ingredient said salt and to processes for their preparation.
US20110262378 Rifaximin Complexes There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex, and therapeutic uses of the complex.
US20080207631 Administering adatanserin; analgesics; Parkinson's disease; amyotrophic lateral sclerosis; vision defects; antiepileptic agents; antihypoxic agents Adatanserin is useful for treating neurodegenerative disorders, chronic pain, and other disorders associated with dysfunctional glutamate release. Methods of treating the same comprise administering a therapeutically effective amount of adatanserin or a pharmaceutical salt thereof, to a patient in need of said treatment.
CN101912354A Composition and application thereof The invention provides a composition. The composition contains oxytropis falcate bunge, Asian rhubarb and vitamin E. The invention also relates to application of the composition to cosmetics and application to preparation of a medicament for repairing damaged skin. Experiment results show that products containing the composition of different concentration can be used for nursing of daily normal skin so that the skin becomes smooth and moist, wrinkles are remarkably removed and pouches are promoted; the products for removing blains can thoroughly remove the blains and do not leave blain imprints; the products are used for sensitive skin for recovery; and the products are used for eliminating skin inflammation and swelling caused by operation, cosmetics, medicaments, radiation and the like. Moreover, the composition provided by the invention is stable, has safe use and no side effect, and can be used for a long term.
US20110076285 Methods and Compositions For Treatment of Ocular Fibrosis Disclosed herein are methods and compositions for treatment of ocular fibrosis, as occurs, for example, during the treatment of glaucoma by trabeculectomy. Compositions comprise modulators of the activity of one or more lysyl oxidase-type enzymes (e.g., LOX, LOXL2), and the methods include methods for making the modulators and methods for administration of the modulators to a subject in need thereof.
WO2006072562A1 Treatment of hcv disorders S1P receptor agonists are useful for the treatment of hepatitis C or chronic hepatitis C (HCV).
US20060182801 Sequestered antagonist formulations Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact, such that the ratio of the mean Cmax of the antagonist after single dose oral administration of the dosage form after tampering to the mean Cmax of antagonist after single dose oral administration of an intact dosage form is at least 1.5:1.
EP2089025A1 Thuggacin-type macrolide antibiotics and their use as antimycobacterial agents The invention provides novel Thuggacin-Type macrolide compounds which form rearrangement products forming a lacton bond to different carbon atoms. The novel compounds can be produced by fermentation of Sorangium cellulosum and Chondromyces crocatus and can be isolated by adsorption and chromoatograhic processing steps. The compounds are found to have antibiotic activity. The invention also relates to Thuggacin A, Thuggacin B, Thuggacin C, 13-Methyl-Thuggacin A, Thuggacin CMC-A, Thuggacin CMC-B and Thuggacin CMC-C AS Antimycobacterial Agents.
CA2642778A1 The use of deferiprone and methods to treat and/or prevent friedreich ataxia resulting from intracellular mishandling of iron A therapeutically effective amount of deferiprone or deferasirox or physiologically acceptable salts thereof for the prevention, stabilization, treatment, or reversal of iron-induced FRDA disease in patients resulting from mitochondrial iron-induced damage to preferentially reduce the iron stores in the mitochondria. Also for the treatment of other conditions affecting the brain where a key element in the generation of the resultant pathology is the intracellular mishandling of iron.
US20110184027 Tissue selective stearoyl-coa desaturase 1 inhibitors and cell based screening assay for their identification The present invention provides a method of treating a disorder treatable by administering a therapeutically effective amount of a tissue selective Stearoyl-CoA Desaturase 1 (SCD-1) modulator to a subject. In one embodiment, the present invention provides a method of treating a disorder treatable by administering a pharmaceutically effective amount of a tissue selective SCD-1 inhibitor to a subject. The invention also provides whole cell based screening assays to identify agents that selectively modulate the activity of SCD-1. This invention further provides whole cell based screening assays to identify agents that differentially inhibit SCD in different body tissues.
EP2252601A1 Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1 This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie),(If), (Ig), (Ih), (Ii), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
CN102973558A Use of matrine in anti- influenza virus drug preparation The present invention discloses a new use of matrine. Experiments of the present invention confirm that the matrine has relatively good inhibitory effect on avian influenza virus. Anti-avian influenza virus drugs are prepared by using the compound and salts thereof as active ingredients. The antiviral drugs can be used for clinical prevention and treatment of diseases caused by the avian influenza virus, having major significance for the livestock breeding industry and public health. In addition, China is rich in herbal resources, so industrial production of the drug is feasible. According to the invention, matrine and matrine hydrochloride have great practical significance and broad application prospects in the medical and bio-pharmaceutical fields, especially in the anti-avian influenza virus drug preparation field.
CN1939288A Composite acne-inhibiting pellicle A medical filming agent for suppressing the generation of scar on wound and improving the healing quality of wound is proportionally prepared from hyaluronic acid, epidermal growth factor and filming agent.
EP0930877B1 D-methionine to reduce the toxicity of platinum-containing anti-tumor compounds Methods of preventing or reducing hearing or balance loss, damage to ear cells, weight loss, gastrointestinal toxicity, neurotoxicity, alopecia, and prolonging survival in patients undergoing treatment with therapeutically effective amounts of platinum-containing chemotherapeutic agents such as cisplatin are provided. These methods comprise administering an effective amount of a methionine protective agent, such as D-methionine, prior to, simultaneously with, or subsequently to administration of the platinum-containing chemotherapeutic agent. Combinations of these time periods can also be employed.
WO2013111105A1 Imidazopyrrolidinone compounds The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
WO2011117449A1 Enantiomers of benzoheteroepine derivatives and use thereof as anti-carcinogenic agents The invention relates to enantiomers of benzoheteroepine compounds, specifically (R)-9-[1-(p-nitrobenzenesulfonyl)-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-il]-2,6-dichloro-9H-purine and (S)-9-[1-(p-nitrobenzenesulfonyl)-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-il]-2,6-dichloro-9H-purine. The invention also relates to the use thereof as drugs, preferably for the treatment of different types of neoplasms.
US8436019 Sulfonyl-piperidin-4-yl methylamine amide analogs as GlyT1 inhibitors, methods for making same, and use of same in treating psychiatric disorders In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
WO2008125901A3 2-methylene-1alpha,25-dihydroxy-18,19,21-trinorvitamin d3 and uses thereof Compounds of formula I are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
CN102119916A Liquid oxygen in-situ forming gel and preparation method and application thereof The invention relates to liquid oxygen in-situ forming gel and a preparation method and application thereof. The liquid oxygen in-situ forming gel comprises the following materials in percentage by weight: 10 to 40 percent of poloxamer, 0.001 to 1 percent of nano silver and 59 to 89.4 percent of solvent. The preparation method comprises the following steps of: adding water into the poloxamer, stirring uniformly, swelling and defoaming to obtain a medicinal base material, adding the nano silver into the base material and stirring uniformly. The liquid oxygen in-situ forming gel can be used for treating vaginitis, rhinitis, otitis and skin tinea diseases. The poloxamer is taken as a temperature sensitive material, and the in-situ forming gel can reside in a human body for more than 20h, so that a medicine taking frequency can be reduced, the compliance of a patient can be improved, a pharmacological treatment effect can be enhanced, and toxic and side effects can be lowered.
CN103159618A 4-carbonyl-2-butene acid compound and purpose thereof The invention provides a 4-carbonyl-2-butene acid compound with good inhibition activity against PA_N. The compound has a general formula (I), wherein R1 represents C1-C4 alkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; and R2 represents hydroxy or substituted amino. The invention also relates to a medicine composition with the compound as an active component, and an application of the compound and the medicine composition provided by the invention in treating influenza.
CN1583746A Methylamino-pterin derivative with inhibiting nitric oxide synthetase function This invention relates to methylaminopterin derivatives with 4-amino structure modified, which inhibit effect of nitrogen monoxide synthetase and growth of tumors. They have wide anti-cancer spectrum and little toxic side effect so as to be used in preparation of medicines for tumors, cancers, arthritis and intestinal diseases as well as chemicals for birth control.
US20110027321 Chlamydia Vaccine Comprising HtrA Polypeptides The present invention provides vaccine compositions useful in prevention and treatment of Chlamydia sp. (e.g., C. trachomatis or C. pneumoniae) infection. Provided are polypeptide vaccine antigens comprising Chlamydia HtrA-derived sequences, including epitopic fragments, analogs, derivatives, and variants. Also provided are a method for inducing an immune response to a subject against Chlamydia infection, a method for preventing Chlamydia infection, or a method for treating a disease or symptom caused by or resulting from infection with Chlamydia, for instance, C. trachomatis or C. pneumoniae. In one embodiment, the present invention is drawn to C. trachomatis HtrA, which induces a cellular immune response and imparts partial protective immunity in vivo.
WO2008053341A3 Bridged bicyclic indazoles as cannabinoid receptor ligands The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).
CN101433513A Semi-interpenetrating network polymer gel for oral colon-specific drug release system and preparation method thereof The invention discloses semi-interpenetrating network polymer gel for oral colon specific drug delivery and a preparation method therefore. The gel comprises the following chemical components: 66.7 to 89.3 weight percent of acrylic acid or methacrylic acid and 8.9 to 28.2 weight percent of polysaccharide in composition of gel polymer, and 1.8 to 6.7 percent of N, N-methylene-bisacrylamide. The preparation method uses water as a medium, persulfate salt and reducing agent as an initiation system, and the N, N-methylene-bisacrylamide as cross linker to synthesize polyacrylic acid and polysaccharide semi-interpenetrating network gel at room temperature, so as to achieve embedding drug for treating colonitis and colon cancer or protein drug. The gel has the characteristics of safety and non-toxicity, high embedding rate for the drug, rich raw material sources, low cost, and low temperature for synthesizing the gel, does not lead the protein drug to lose activity, and the like.
US20100120708 Combination therapy comprising ZD6474 and gemcitabine for anti-cancer therapy The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of ZD6474 in combination with gemcitabine; to a pharmaceutical composition comprising ZD6474 and gemcitabine; to a combination product comprising ZD6474 and gemcitabine for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and gemcitabine; to the use of ZD6474 and gemcitabine in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.
WO2010133885A1 Novel pyrimidine derivatives and their use in the treatment of cancer and further diseases The invention concerns compounds of Formula (I): wherein L1, R1, R2, R3, R4 and X are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of disease, for example cancer.
CN101496852A Medicament for treating protrusion of lumbar vertebral disc and method for producing the same The invention relates to a medicament for treating lumbar intervertebral disc protrusion and a preparation method thereof. The preparation method comprises the following steps: firstly, selecting frankincense, myrrh, cutch, angelica dahurica, acutangular anisodus root, pendulous monkshood root, unprocessed radix aconiti, unprocessed semen strychni, unprocessed kusnezoff monkshood root, datura flower seed, thelepus, asarum pearl powder, pangolin, fructus piperis longi, lucid ganoderma and blood flower in terms of each 200 to 400 grams, and then cleaning the raw materials; soaking the cleaned raw materials into 25,000 grams of sesame oil for 15 days; then heating the mixture for 5 hours by mild fire, and keeping the temperature of the oil to between 80 and 100 DEG C; heating the mixture for 10 minutes by intense fire, and keeping the temperature of the oil to between 200 and 400 DEG C; then removing decoction dregs; repeating the steps of mild fire heating, intense fire heating and decoction dreg removing for three times; finally heating the decoction for 60 minutes by the intense fire, and keeping the temperature of the oil to between 200 and 400 DEG C; later adding 12,500 grams of massicot into the decoction; and after the temperature of the oil is reduced to room temperature, adding 6 to 12 grams of musk into the decoction, and evenly stirring the mixture to form an ointment for use. The medicines are used together for treating both symptoms and root causes and outstanding wound; and the ointment pasted on the afflicted part has long-acting efficacy and high cure rate for treating the lumbar intervertebral disc protrusion.
DE102005061720B3 Preparing optically active omeprazole enantiomers, useful to treat stomach diseases, comprises oxidizing prochiral sulfide compound with oxidizing agent in presence of titanium complex catalyst and reacting the catalyst with chiral diols Preparing optically active enantiomers or an enantiomeric form of omeprazole compound (I) comprises oxidizing a prochiral sulfide compound (II) with an oxidizing agent in the presence of an organic solvent and titanium (IV) complex catalyst; and reacting the complex catalyst with a chiral (R, R) or (S, S)-1,2-arylethane-1,2-diol. Preparing optically active enantiomers or an enantiomeric form of omeprazole compound of formula (I) comprises oxidizing a prochiral sulfide compound of formula (II) with an oxidizing agent in the presence of an organic solvent and titanium (IV) complex catalyst; and reacting the complex with a chiral (R, R) or (S, S)-1,2-arylethane-1,2-diol. Either R1>-R4>H, alkyl, alkoxy, halo, alkoxyhalo, alkylcarbonyl, alkoxycarbonyl, oxazole or trifluoroalkyl; or R1>R2>R3>R4>optionally substituted ring structure; R5>H with a condensed ring system or a ring system with Ar1>; Ar1>pyridine compound of formula (III) or a benzene compound of formula (IV); R6>-R8>H, alkyl, alkylthio, alkoxy or halo (optionally substituted by alkoxy, dialkoxy, dialkylamino, piperidine, morpholine, halo, phenylalkyl, or condensed ring system with R5>); and R9>, R10>H, halo, trifuloromethyl, alkyl or alkoxy. [Image] [Image] - ACTIVITY : Antiulcer. No biological data given. - MECHANISM OF ACTION : None given.
WO2008089628A1 A nanoparticle of glucidamin for treating tumor and preparation method thereof A nanoparticle of glucidamin derived from organism for treating tumor and preparation method thereof, wherein the viscosity-average molecular weight of glucidamin is in the range of 1×103-9×105, and the amount of free amino in the glucidamin is in the range of 50%-100% based on the total amino. The preparation method of the nanoparticle comprises steps listed below: (1) adding the glucidamin possessing one or more molecular weight into thin acid solution at 20-60°C to form saccharan solution, wherein the content of saccharan in solution is in the range of 0.1%-5% by weight; (2) adjusting the pH of the solution to 6-9 in order to form emulsion of microparticle; (3) separating the microparticle from the emulsion, dried at low temperature to obtain the nanoparticle of glucidamin for treating tumor. The nano-class glucidamin can enhance their activity against tumor. The particle diameter of glucidamin nanoparticle prepared by the method disclosed in the present invention exhibits homogeneous distribution, meanwhile, the nanoparticle is easy to be separated and purified.
WO2009072581A1 Lactam compound or salt thereof, and ppar activator Disclosed is a compound having a lactam skeleton or a salt thereof, which is useful as a PPAR activator. Specifically disclosed is a lactam compound represented by formula (1) or a salt thereof. (1) wherein R1 represents a halogen, a hydrocarbon group, a carboxyl group or the like; Z1 represents an arene ring or a hetero ring; Z3 represents an alicyclic or aromatic hydrocarbon ring; Z2 represents a 5- to 6-membered ring containing a nitrogen atom; X1 represents a C, O, S or N atom, a group -N-C(=O)- or a group -C(=O)-N-; R2 represents a hydrogen atom or an alkyl group which may have a substituent; R3 and R4 independently represents a single bond or a bivalent aliphatic hydrocarbon group, provided that at least one of R3 and R4 represents an aliphatic hydrocarbon group; X2 and X3 independently represent a single bond, an O or S atom, an imino group or the like; A1 represents a single bond or a phenylene group which may have a substituent; Y1 represents a hydrogen atom, a halogen atom, a carboxyl group or the like; a represents an integer of 0 to 5; b represents an integer of 0 to 2; and c represents an integer of 1 to 3.
US20110082194 Synergistic Anticoagulant Composition A composition is provided that, when utilized in combination with warfarin, greatly improves the anticoagulant effects of warfarin in mammalian subjects. The composition is a compound having a naphthohydroquinone ring system substantially similar to the ring system of the reduced form of vitamin K1 and has the general formula: where R1 and R4 are hydrogen or acyl, R2 is a saturated or unsaturated alkyl group with up to 6 carbons, and R3 is a saturated or unsaturated alkyl group with up to 20 carbons, or R2 and R3 are part of a cyclic or polycyclic ring system.
WO2011088055A3 Methionine aminopeptidase 2 (metap2) inhibitors for treating cardiovascular or cerebrovascular disorders The invention generally relates to methods of treating a patient having, and/or at risk of, cardiovascular or cerebrovascular disorders. Such methods may include administering a MetAP2 inhibitor at a dose that does not substantially modulate angiogenesis.
CN103764657A Hydroxymethylaryl-substituted pyrrolotriazines as ALKL inhibitors This invention relates to novel 5-[(hydroxymethyl)aryl] -substituted pyrrolo[2, 1-f][1, 2, 4] triazin-4-amines of formula (I), to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating angiogenesis-related disorders, in particular angiogenesis-related ocular disorders.
CN101473832B Novel environment-friendly type disinfecting liquid The invention relates to a disinfectant, in particular to a disinfectant containing aldehyde derivatives and tridecane quaternary ammonium salt derivatives. The disinfectant comprises 1 part to 5 parts of hexamethylene tetramine and 1 part of benzalkonium bromide according to the parts by weight. The disinfectant has the advantages of simple preparation, excellent disinfection effect, long periodof validity, excellent environmental-protection performance, low irritability, no toxic and no harm to the human body and the animals and the like; and the disinfectant can be widely applied to disinfection and sterilization for air, various tools, hand parts and equipment pipelines.
CN1823839A Vitamin microelement mineral calcium nutritire product for preventing and treating nightblindness and its manufacturing method A nutrient used as both medicine and food for preventing and treating nyctalope is prepared from vitamins, trace elements and Ca. Its preparing process is also disclosed.
US20060040940 Imidazopyridines pyrimidines and triazines for enhancing cognition as gaba-a-alphas 5 receoptor subtype ligands The present invention provides a pharmaceutical composition providing a compound of formula I or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable excipient: (I), in which: X and Y independently represent CH or N, with the proviso that if X is CH then Y is also CH; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, —CO2Ra, —CONRaRb or CRa═NORb; Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; V and W are independently selected from H, halogen, C11-6alkyl, OH and C-1-6alkoxy; Z represents H, halogen, CN, NO2, CF3, OCF3, CF2H, SCF3, R2, OR3, SR3, (CH2)pN(R3)2, O(CH2)pN(R3)2, SO2R2, SO2N(R3)2, COR4, CO2R3, CON(R3)2, NHCOR4, NR1(CH2)nheteroaryl or O(CH2)nheteroaryl the heteroaryl is optionally substituted by one, two or three groups chosen from C1-6alkyl, benzyl, (CH2)pN(R3)2, halogen and CF3, R1 is C1-6alkyl, where n is 1 or 2 and p is 0, 1 or 2; with the proviso that at least one of V, W and Z is other than H; R2 represents C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-4alkyl, C2-6alkenyl, C2-6alkynyl or heteroaryl, any of which may bear a substituent selected from halogen, CN, NO2, CF3, OCF3, CF2H, SCF3, OH, C1-4alkoxy, C1-4alkoxycarbonyl, amino, C1-4alkylamino, or di(C1-4alkyl)amino; R3 represents H or R2; or two R3 groups bonded to the same nitrogen atom may complete a 5-7 membered nonaromatic heterocyclic ring; and R4 represents R3 or heteroaryl; the compounds are ligands for GABA-A receptors containing the alpha 5 subtype and thus are useful for enhancing cognition in individuals suffering from conditions such as Alzheimer's Disease.
CN101627978B Glipizide sustained-release capsule formulation and preparation method thereof The invention relates to a glipizide sustained-release capsule formulation and a preparation method thereof. The glipizide sustained-release capsule formulation contains three glipizide sustained-release pillers with different release periods, wherein the glipizide sustained-release pillers respectively include conventional glipizide sustained-release pillers and glipizide time-delay sustained-release pillers in the following percentage by weight: 20-80 percent of the glipizide sustained-release pillers, 10-50 percent of glipizide 4-hour time-delay sustained-release pillers and 5-30 percent of glipizide 8-hour time-delay sustained-release pillers. A release curve of the glipizide sustained-release capsule formulation is more similar to a physiological change curve of the blood sugar concentration of human bodies, and release peaks of glipizide are respectively generated after the glipizide sustained-release capsule formulation is orally taken, 4 hours later and 8 hours later, corresponding to three meals a day, which are orally taken by ordinary people, thereby better controlling the blood sugar levels, reducing the blood sugar fluctuation of diabetics and bringing better treatment effect to patients.
CA2200084C Use of aromatic halides for treating mammalian cell proliferation The present invention provides methods and product for inhibiting mammalian cell proliferation. Compounds that are anti-mycotics and that inhibit the Ca++-activated potassium channel of erythrocytes have been modified for use in the present invention by removing the imidazole group. Such modified compounds typically have at least aromatic groups separated from one another by not more than five atoms, and more typically not more than three atoms. At least one of the aromatic groups is substituted with a chlorine or another functionality with an overall net negative charge. The compounds can be used in connection with, inter alia, treatments for cancer, treatments for arteriosclerotic conditions, treatments for angiogenic conditions and other cell proliferative disorders.
WO2008095852A1 Bronchorelaxing arylamides The invention relates to novel molecules having the general formula (I), and which molecules are useful to manufacture a medicament to treat a disorder or disease characterized by bronchoconstriction.
WO2009095210A1 Composition comprising an antacid and a h2-antagonists The present invention relates to a stable solid composition comprising an antacid and a H2- antagonist without unpleasant or bitter taste, its process for preparation and its use for treating and preventing gastric disorders.
CN1883508A Anti-dust nasal cleanser Disclosed is a nasal cavity cleaning liquid for preventing dust-in, which is prepared from the following raw materials (by weight percent): sea salt 3.0-5.0%, glycerol 0.5-1.5%, albumen candy 0.05-0.2%, water-soluble pearl powder 0.05-0.2%, lemon acid 0.05-0.2%, lemon peppermint perfume compound 0.01-0.05%, menthol 0.005-0.01%, EDTA-2Na 0.01-0.04% and balancing water.
WO2011079764A1 Solid formulation of eszopiclone and the preparation method thereof A preparation method of a solid formulation of eszopiclone and the solid formulation prepared by the method are disclosed. Said method comprises dissolving eszopiclone in an acidic solution containing an acidifier to obtain an acidic liquid of the drug; following, homogeneously mixing an alkalizer, excipients and the acidic liquid of the drug and carrying out wet-granulation; wherein the alkalizer is a reagent that makes the acidity of the mixture liquid of the alkalizer and the acidic liquid less than the acidity of the acidic liquid of the drug.
US20060142556 Modulation of oligonucleotide CpG-mediated immune stimulation by positional modification of nucleosides The invention provides methods for modulating the immune response caused by CpG dinucleotide-containing compounds. The methods according to the invention enables both decreasing the immunostimulatory effect for antisense applications, as well as increasing the immunostimulatory effect for immunotherapy applications.
US20080214503 Diethyl[2-({[7-[(4-fluorophenyl)methyl]-4-hydroxy-3-({[2-(methyloxy)ethyl]amino}carbonyl)-2-oxo-1,5-naphthyridin-1(2H)-yl]acetyl}amino)ethyl]phosphonate; alone or with a second enzyme inhibitor The present intention features compounds that are HIV integrase inhibitors and may be useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
EP1749528A1 Pharmaceutical combinations containing a mu opioid agonist and an inhibitor of NO production The present invention relates to compositions and methods for treatment and/or prevention of oedema, pruritus and hyperalgesia often associated with activation of peripheral sensory nerves (neurogenic inflammation). The compositions, which may be formulated for topical and local administration, contain relatively selective µ-opioid agonists that are substantially devoid of central nervous system effects, in combination with inhibitors of NO production, preferably, but not limited to, inhibitors of nitric oxide synthase (NOS), and in particular non-selective inhibitors, or relatively selective inhibitors of the neuronal NOS (nNOS) and inducible NOS (iNOS) isoforms.
CN102144978A Acetylcysteine granule and preparation technology thereof The invention discloses an acetylcysteine granule and a preparation method thereof, which belong to the new technical field of pharmaceutical preparation, and relates to a new composition of the acetylcysteine granule and the perpetration technology thereof. In the new composition and the preparation technology thereof, the granule mainly consists of acetylcysteine, acrylic resin, mannitol, aspartame and orange essence, and weight ratio of the main constituents is 10:1-50:2-200:0-1:0-1. After being coated with the acrylic resin, the acetylcysteine is mixed with the dry mannitol granule, the aspartame and the orange essence to prepare the acetylcysteine granule; and the prepared acetylcysteine granule has obviously improved stability in wet environment, and the taste of the acetylcysteine granule is greatly improved.
US20110243964 Treatment of orthopedic conditions Methods, compounds, compositions, kits and articles of manufacture comprising anti-connexin agents for treatment of orthopedic disorders, diseases, or conditions, and improving recoveries and outcomes of orthopedic procedures or surgeries.
CN102146014A Method for extracting squalene by using camellia oleosa seeds as raw materials and tea oil and squalene soft capsules The invention discloses a method for extracting squalene by using camellia oleosa seeds as raw materials and tea oil and squalene soft capsules and relates to the technical field of biomedicine. The extraction method comprises the following process flows of material preparation, grinding, leaching, concentration, methyl esterification, complexant-borax reaction, macroporous resin chromatographic separation and purification, concentration, extraction, washing, concentration, preparation of squalene crude oil and supercritical carbon dioxide extraction, so that squalene essential oil with the squalene content of more than or equal to 80 percent is obtained. The tea oil and squalene soft capsules are prepared from the following raw materials in percentage by weight: 87 to 90 percent of squalene essential oil with the squalene content of more than or equal to 80 percent, 3 to 5 percent of polyethylene glycol 400, 2 to 3 percent of beewax and 2 to 5 percent of phospholipid. The raw material resources are wide. The prepared tea oil and squalene soft capsules not only can be used for medicine, but also can be used for food therapy, are particularly suitable for administration of treatment and food therapy of patients suffering from hepatitis, fatty liver, acute and chronic inflammation, tumor, chemotherapy, diabetes mellitus and cardio-cerebrovascular disease and have no toxic or side effects.
CA2739209A1 Use of 3,11b-cis-dihydrobenazine in the treatment of dementia and associated cognitive deficit A 3,11b cis-dihydrotetrabenazine or a pharmaceutically acceptable salt thereof for use in the treatment of dementia.
WO2014042263A1 Novel renin inhibitor The invention provides a nitrogen-containing saturated heterocyclic compound useful as a renin inhibitor. A compound represented by formula [I] (in the formula, R1 represents a cycloalkyl or alkyl, R22 represents an optionally substituted aryl or the like, R represents a lower alkyl group, R3, R4, R5, and R6 are the same or different and represent a hydrogen atom, optionally substituted carbamoyl, optionally substituted alkyl, or alkoxycarbonyl) or a pharmaceutically acceptable salt thereof.
WO2006021660A8 Use of at least one conjugated triene-containing fatty acid for preparing a medicine for treating inflammation The invention concerns the use of at least one conjugated triene-containing fatty acid for preparing a medicine for treating inflammation selected among the group consisting of alpha-eleostearic acid, catalpic acid, calendic acid, jacaric acid, licanic acid and beta-eleostearic acid for making a medicine for treating inflammatory diseases and/or metabolic disorders following an inflammation. The inflammatory diseases and/or metabolic disorders following an inflammation may be skin cancers, sun burn, benign summer light eruption, allergic and/or irritative reactions, gingivitis and periodontitis, vulvitis and vaginitis or arthritis and arthrosis. The medicine also enables healing to be promoted. Said fatty acid conjugates can also be used in the cosmetic treatment of cellulitis.
WO2008077649A1 Pyrido(3,2-d)pyrimidines useful for treating viral infectons 2-amino-pyrido(3,2-d)pyrimidine derivatives with a specific substitution pattern on positions 4 and 6 of the core structure are useful in the treatment or prevention of an infection due to a virus from the Flaviviridae family, especially HCV, when administered to a patient in a therapeutically effective amount.
EP1397366B1 Novel ligand for nicotinic acetylcholine receptors useful in therapy A compound having the formula (I): and any pharmaceutically-acceptable salts thereof, and their uses in therapy andcompositions containing them.
CN101678031A Formulations containing triazinones and iron The invention relates to the simultaneous application of triazines such as toltrazuril, ponazuril or diclazuril and iron compounds in a formulation for controlling coccidia infections and iron deficiencies in animals and humans.
WO2009108332A1 INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE TYPE 1 This invention relates to novel compounds of the Formulae I or II and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD l in mammals.Formula (I).
WO2008074982A1 Pyrazole derivatives as modulators of cannabinoid receptor Compounds of formula (I) suppress the normal signalling activity of CB1 receptors, and are useful in the treatment of, for example obesity or overweight formula (I): wherein A1, A2, A5, A6, R1, R2, R3, and X are as defined in the claims.
CN103006607A Lansoprazole enteric-coated tablet and method for preparing same The invention discloses a lansoprazole enteric-coated tablet which comprises lansoprazole, a stabilizer, an antioxidant, a filler, a disintegrant, a lubricant and an appropriate amount of adhesive, wherein the lansoprazole servers as an active component. The lansoprazole is made into the tablets for treating peptic ulcer. The lansoprazole enteric-coated tablet is characterized in that the alkaline stabilizer is adopted in the prescription so that a weak-alkaline microenvironment can be formed in the lansoprazole enteric-coated tablet and the degradation of medicament in the presence of other accessories and under the acidic condition is inhibited, and the antioxidant is added to the prescription so that the oxidation and the degradation of the medicament in the air are inhibited and the quality of the medicament is guaranteed. During production, the active pharmaceutical components and a part of accessories are micronized so that the particle size of the active pharmaceutical components is reduced and the solubility of the medicament is improved. Due to the adoption of the enteric coating process, the degradation of the medicament in the gastric acid is avoided, the targeted release of the medicament is guaranteed, and the bioavailability of the medicament is improved. Due to the optimization of the prescription and the process, the stability of the medicament during production is guaranteed, and the quality of the production is improved.
WO2005039599A1 Matrix metalloprotease inhibitor containing polylactic acid mixture It is intended to provide a novel matrix metalloprotease inhibitor by evaluating the matrix metalloprotease inhibitory effect shown by a cyclic and/or chain polylactic acid mixture. Namely, a matrix metalloprotease inhibitor containing a cyclic and/or chain polylactic acid mixture having a degree of condensation of from 3 to 20.
US20050085548 Administering mixture of arginine and reductase inhibitase; therapy for endothelial cell diseases; hypotensive agents; cardiovascular disorders brain disorders A therapeutic mixture comprised of L-arginine and inhibitors of Hmg-CoA-Reductase is disclosed for the treatment of diseases related to endothelial dysfunction, wherein the endothelial dysfunction is relieved by stimulating the constitutive form of nitric oxide synthase (cNOS) to produce native nitric oxide (NO).
WO2007062595A1 Bismuth hyaluronate, the preparation method and the use theirof Bismuth hyaluronate, characterized in that the bismuth content in dried product is 0.5%~40% with 20%~45% uronic acid. The preparation method of bismuth hyaluronate comprises: taking reaction between soluble hyaluronic-acid salt and bismuth salt in basic aqueous solution, depositing, filtering, desalting, dewatering, and drying. This product can be used in producing the medicament for treating and preventing gastrointestinal disease and used in preparing health foods, and especially in the medicament for treating gastrointestinal ulcers with better curative effect to similar products shown by animal testing.
EP1569636A4 Use of equol for treating androgen mediated diseases Equol (7-hydroxy-3(4’hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5α-dihydrotestosterone (DHT) in vitro and in vivo. Equol can bind circulating free DHT and sequester it from the androgen receptor, thus altering growth and physiological hormone responses that are regulated by androgens. These data suggest a novel model to explain equol’s biological properties, The significance of equol’s ability to specifically bind and sequester DHT from the androgen receptor have important ramifications in health and disease and may indicate a broad and important usage for equol in the treatment and prevention of androgen-mediated pathologies. Thus, equol can specifically bind DHT and prevent DHT’s biological actions in physiological and pathophysiological processes.
US20090076065 Deuterium-enriched mk-0812 The present application describes deuterium-enriched MK-0812, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2014135244A1 Triazolo[4,5-d]pyrimidine derivatives for the treatment of diseases such as cancer Compounds of the formula I, in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
CN103405640A Preparation method of bowel clearing granules before late pregnancy labor induction The invention discloses a preparation method of bowel clearing granules before late pregnancy labor induction, which aims to solve the problem of bowel clearing before late pregnancy labor induction. The invention is characterized by comprising the following active pharmaceutical ingredients in parts by weight: Horseweed herb, Fructus Cinnamomi, ternate buttercup root, Trachelospermum jasminoides, Asarum maximum Hemsl., rhizoma polygonati, fructus psoraleae, dried orange peel, sunflower, Turbo cornutus Solander, plant soot and magnesium sulfate. The preparation method comprises the following steps: (1) extracting volatile oils from fructus psoraleae, Fructus Cinnamomi and Asarum maximum Hemsl. coarse powders for later use; (2) pulverizing Turbo cornutus Solander and plant soot into fine powders for later use; (3) decocting horseweed herb, ternate buttercup root, Trachelospermum jasminoides, rhizoma polygonati, sunflower and dried orange peel with water 2 times, filtering, merging the filtrates, concentrating the filtrate, adding ethanol to precipitate, taking the supernatant, recovering the ethanol, and concentrating to obtain a thick paste; and (4) adding the volatile oils obtained in the step 1, the fine powders obtained in the step 2, and magnesium sulfate into the thick paste obtained in the step 3, stirring uniformly, granulating, and drying. The clinical experiment proves that the invention has the characteristic of favorable bowel clearing effect before late pregnancy labor induction, and is worthy of clinical application and popularization.
US20100297224 NSAID Dose Unit Formulations with H2-Receptor Antagonists and Methods of Use The present invention generally relates to pharmaceutical unit dosage forms of NSAIDs and H2-receptor antagonists, in which the H2-receptor antagonist is formulated so as to be released in a sustained manner over a predetermined period of time so as to maintain gastric pH above a desired level for a duration of time. The NSAID may then be formulated for immediate release. The pharmaceutical unit dosage forms may be administered to subjects susceptible to the development of NSAID induced gastric and/or duodenal ulcers, as the sustained release H2-receptor antagonist is formulated so as to maintain the gastric environment above the pH levels where NSAID-induced ulceration typically occurs.
CN103393655A Application of Sarcaboside B to medicament for treatment and prevention of oral ulcer The invention relates to application of Sarcaboside B to preparation of medicaments for the treatment or prevention of oral ulcer. The application of Sarcaboside B to preparation of medicaments for the treatment of oral ulcer involved in the invention is disclosed for the first time. As the Sarcaboside B has a novel skeleton type and unimaginably strong activity in treatment of oral ulcer, no other compound can give any enlightenment. The invention has outstanding substantive distinguishing features and makes substantial progress in the treatment of oral ulcer.
CN101204379A Ambroxol cefadroxil dispersible tablets The invention discloses a compound dispersible tablet, which contains active components of cefadroxil and ambroxol hydrochloride, and the pharmacologically-acceptable excipient. The compound dispersible tablet is used for curing the upper respiratory tract infection.
CN102106832A Ketoconazole nanometer suspension freeze-dried powder and preparation method thereof The invention discloses ketoconazole nanometer suspension freeze-dried powder and a preparation method thereof. The ketoconazole nanometer suspension freeze-dried powder is prepared from the following components in part by mass: 1 part of ketoconazole medicinal powder, 1.5 to 4 parts of surfactant and 0.5 to 2 parts of freeze-dried auxiliary material. The preparation method comprises the following steps of: dissolving ketoconazole in mixed solvent of organic solvent and water-soluble organic solvent, adding water in which the surfactant is dissolved, stirring until the mixture is clarified, adding the freeze-dried auxiliary material, stirring until the mixture is clarified, putting into a refrigerator at the temperature of below 20 DEG C, and freeze drying for over 48 hours to prepare the ketoconazole nanometer suspension freeze-dried powder. In the ketoconazole nanometer suspension freeze-dried powder, ketoconazole medicinal granules are reduced to a nanoscale, so the dissolution rate of the ketoconazole in the water is improved greatly, and the antifungal effect of the ketoconazole is fully played. The freeze-dried powder can be applied to the preparation of freeze-dried powder injection, soft capsules, oral liquid, tablets, gel, emulsifiable paste and other liquid and solid formulations which are used for treating superficial and deep fungal infection.
EP1731153A1 Immediate-release and high-drug-load pharmaceutical formulations of non-micronised (4-chlorophenyl)¬4-(4-pyridylmethyl)phthalazin-1-yl| and salts thereof The invention relates to immediate-release and high-drug-load solid pharmaceutical formulations comprising non- micronized (4-chlorophenyl)[4-(4-pyridylmethyl)-phthalazin-1-yl] as well as pharmaceutically acceptable salts thereof.
EP0904283B1 Human netrin-1 Specific netrin proteins, nucleic acids which encode netrin proteins and hybridization reagents, probes and primers capable of hybridizing with netrin genes and methods for screening chemical libraries for lead compounds for pharmacological agents useful in the diagnosis or treatment of disease associated undesirable cell growth are provided. An exemplary screen involves forming a mixture comprising a recombinant netrin protein, a natural intracellular netrin protein binding target and a candidate pharmacological agent; incubating the mixture under conditions whereby, but for the presence of said candidate pharmacological agent, said netrin protein selectively binds said binding target; and detecting the presence or absence of specific binding of said netrin protein to said binding target.
US20080102037 Stable pharmaceutical budesonide preparation for producing propellant-free aerosols The invention relates to ethanol-containing pharmaceutical preparations for the production of propellant-free aerosols.
US6838461 Psychological disorders; schizophrenia; Alzheimer's disease; Parkinson's disease; Huntington's disease; cardiovascular disorders; hypotensive agents; side effect reduction Compounds of the formula I in which R1, R2, R4 and R5 have the meanings indicated in claim 1, are potent 5-HT2A antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkingson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia, nervous anorexia, premenstrual syndrome and/or for positively affecting compulsive behavior (obsessive-compulsive disorder, OCD).
CN101147730A Constitution of xylitol tablet containing selenium and vitamin E and manufacturing method thereof The present invention relates to a xylitol tablet composition containing selenium and vitamin E and its preparation method, belonging to the field of food, health-care food and medicine. Its main components include selenium, vitamin E, xylitol, binding agent, excipient, additive and coating agent. It is characterized by that its functional components are selenium and vitamin E, its binding agent is acacia gum and its coating agent is xylitol. Its preparation method includes the following steps: pulverizing, mixing, granulating, finishing, tabeleting and packaging.
US20100240580 Azoloarine derivatives, method for the production thereof, pharmaceuticals containing these compounds and the use thereof The invention relates to azoloarine derivatives of formula I wherein R, A, B, D, Y, X, M and W are as defined herein, and their physiologically tolerated salts.
EP2745849A1 Polydeoxyribonucleotides composition and uses thereof Composition comprising polydeoxyribonucleotides (PDRN) and chitosan for stimulating cell proliferation.
EP1803458A1 Use of inorganic salts in the treatment of inflammation The present invention relates to the treatment of inflammation and irritation with non-steroidal compositions containing inert salts including magnesium and potassium salts. More particularly the compositions are used to treat mucosal parts and to provide oral hygiene.
WO2011041907A1 Derivatives of di(phenylpropanoid) glycerol for the treatment of cancer The present invention provides a method for treating a cancer in a subject involving administering to the subject a compound of formula (II) or (II'): wherein R1, R2, R3, R4, R5, R6 and R7 are independently H, OH, alkoxy or alkylcarbonyloxy, or a pharmaceutically acceptable salt thereof. Also provided is a compound of formula (II) or (II)', wherein R1 and R2 are independently OH, alkoxy or alkylcarbonyloxy, R3 and R4 are independently H, OH, alkoxy or alkylcarbonyloxy, R6 is H, alkoxy or alkylcarbonyloxy, R5 is H, OH or alkylcarbonyloxy, R6 is H or alkoxy, and R7 is H, or a pharmaceutically acceptable salt thereof.
EP2305677A1 Alkyne-aryl-naphthyridin-4(1h)-one derivatives as type IV phosphodiesterase inhibitor Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation.
CN102309722A Medicinal liquor for treating injury and preparation method of same The invention discloses medicinal liquor for treating an injury and a preparation method of the same. The medicinal liquor is prepared by soaking medicines for the medicinal liquor for treating the injury in white spirit, wherein the medicines comprise borneol, curcuma zedoary, syzygium aromaticum, carthamus tinctorius, radix saposhnikoviae, rhizoma sparganii, Chinese tinospora stem, ardisia crenata, radix zanthoxyli and radix fici simplicissimae root; and the medicinal liquor comprises the following parts of medicines by weight in terms of 900 parts of white spirit by weight: 4-10 parts of borneol, 4-10 parts of curcuma zedoary, 6-12 parts of syzygium aromaticum, 6-12 parts of carthamus tinctorius, 7-15 parts of radix saposhnikovia, 7-15 parts of rhizoma sparganii, 7-15 parts of Chinese tinospora stem, 7-15 parts of ardisia crenata, 10-20 parts of radix zanthoxyli and 10-20 parts of radix fici simplicissimae root. The medicinal liquor has a better growth function of promoting and accelerating the healing of the injury by the combined action of respective medicines, can be used for reducing swelling, relieving pain, relaxing the muscles, and stimulating the blood circulation afterbeing exerted externally, and has better effects for treating diseases such as traumatic injuries and the like.
DE102004008112A1 New 8-aminopiperidinyl-xanthine derivatives, useful for treating e.g. diabetes, arthritis and osteoporosis, are inhibitors of dipeptidylpeptidase-IV 8-(3-Aminopiperidinyl)-xanthine derivatives (I), their tautomers, enantiomers, diastereomers, or mixtures, and salts are new. - 8-(3-aminopiperidinyl)-xanthine derivatives of formula (I), their tautomers, enantiomers, diastereomers, or mixtures, and salts are new. - R = benzyl (optionally substituted), (benzo(1,3)dioxol-5-yl)methyl, 2-(3-cyclopropyloxy-, cyclopropylmethoxy- or cyclobutyloxy-phenyl)-2-oxo-ethyl, 2-oxo-2-(2-(pyridin-3 or 4-yl)phenyl)ethyl, naphthalen-1-ylmethyl ring substituted by 3-cyano, 1,4-dicyano or 2,4-dimethoxy, pyridinylmethyl (optionally ring substituted), ((2,2')bipyridinyl-6-yl)methyl, 2-phenylpyrimidin-4-ylmethyl, 4-phenylpyrimidin-2-ylmethyl, ring-substituted quinolin-2-ylmethyl, ring-substituted isoquinolin-3-ylmethyl, optionally ring-substituted quinazolinylmethyl, quinoxalin-5-ylmethyl, 2,3-dimethylquinoxalin-6-y lmethyl or (1,5)naphthyridin-3-ylmethyl. - The full definitions are given in the DEFINITIONS - Full Definitions Field. - An INDEPENDENT CLAIM is also included for two methods for preparing (I). - ACTIVITY - Antidiabetic; Antiarthritic; Anorectic; Immunosuppressive; Osteopathic; Antilipemic; Antiarteriosclerotic; Cardiant; Hypotensive; Nephrotropic; Antiinfertility; Antiinflammatory. - MECHANISM OF ACTION - (I) are inhibitors of dipeptidylpeptidase-IV (DPP-IV). - The compound 1-(4(4-phenylaminoquinazolin-2-yl)methyl)-3-methyl-7-(2- butyn-1-yl)-8-(3-aminopiperidin-1-yl)xanthine had in vitro IC50 against human DPP-IV of 6 nM.
CN101518654B Method for synthesizing novel preparation capable of carrying glucocorticoid to be used as inflammation targeted drug The invention discloses a method for synthesizing novel preparation capable of carrying glucocorticoid to be used as inflammation targeted drug. The method uses water-soluble N-(2-hydroxypropyl) methaThe invention discloses a method for synthesizing novel preparation capable of carrying glucocorticoid to be used as inflammation targeted drug. The method uses water-soluble N-(2-hydroxypropyl) methausing adverse reaction to normal tissues.using adverse reaction to normal tissues.crylamide polymer as the carrier for carrying the glucocorticoid and comprises the following five steps of synthesizing the inflammation targeted drug formed through the joint of the polymer N-(2-hydrcrylamide polymer as the carrier for carrying the glucocorticoid and comprises the following five steps of synthesizing the inflammation targeted drug formed through the joint of the polymer N-(2-hydroxypropyl) methacrylamide polymer and prednisolone (1): synthesizing polymer N-(2-hydroxypropyl) methacrylamide polymer; (2) synthesizing short peptide chains; (3) synthesizing polymer-peptide chain moxypropyl) methacrylamide polymer and prednisolone (1): synthesizing polymer N-(2-hydroxypropyl) methacrylamide polymer; (2) synthesizing short peptide chains; (3) synthesizing polymer-peptide chain multipolymer; (4) synthesizing leading molecules of the polymer; and (5) synthesizing polymer-peptide chain prednisolone. The novel inflammation targeted drug with excellent performance can orientationultipolymer; (4) synthesizing leading molecules of the polymer; and (5) synthesizing polymer-peptide chain prednisolone. The novel inflammation targeted drug with excellent performance can orientationally carry the prednisolone to inflammatory tissues, particularly the arthritis tissues so that the prednisolone releasing in the arthritis tissues exerts favorable anti-inflammatory effect without caally carry the prednisolone to inflammatory tissues, particularly the arthritis tissues so that the prednisolone releasing in the arthritis tissues exerts favorable anti-inflammatory effect without ca
WO2007065451A1 Means for preventing and treating rhinitis of different ethiology, method for the production thereof, a pharmaceutical composition based thereon and a preventing and treating method The invention relates to the chemico-pharmaceutical industry and can be used for medical practice in a monotherapeutic mode and for the multimodality treatment of rhinitis of different ethiology. Said invention also relates to a disulphide tetralithium salt and to a method for the production thereof consisting in oxidising a starting compound, embodied in the form of a reduced glutathione (η-L-glutamyl-L-cysteinyl-glutaminyl-glicine), by a hydrogen dioxide in the presence of aqueous ammonia, in releasing a free hexapeptide (bis((η-L-glutamyl)- L-cysteinil-bis-glicine) by acidifying the solution with a glacial acetic acid, in converting the acidified form of free hexapeptide in a tetralithium salt, in filtering the solution in vacuum, in stabilising the hexapeptide disulphide bond by exposing the reaction solution to an ultraviolet radiation and in releasing a final product by a liophylic drying method. The inventive means can be used in the form of a medicinal preparation for preventing and treating rhinits of different ethiology, including vasomotor rhinitis. A pharmacological composition containing a disulphide glutathione tetralithium salt, zinc sulphate, hydrogen dioxide, adrenaline and water for injections, dosage forms based on said medicinal composition, for example nasal drops and spray, and a method for preventing and treating nosological forms of acute and chronic infection and allergic diseases of nasal mucous are also disclosed.
EP2656851A1 Semuloparin for improving the survival of patients with cancer The invention relates to an ultra-low molecular weight heparin with an average molecular weight of 2000 to 3000 Daltons, an anti-FXa activity of about 160 U/mg and an anti-Flla activity of about 2 U/mg, in particular semuloparin, for use as a prophylactic antithrombotic agent in cancer patients receiving chemotherapy for locally advanced solid tumors, wherein said use is accompanied by an improval of the survival of patients with locally advanced cancer of the lungs or with a venous thromboembolism risk score equal to or greater than 3.
WO2012055020A1 Thermosensitive liposomes In one aspect, the present invention provides a thermosensitive liposome comprising a lipid bilayer comprising 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) and a compound of formula (I): C17H35(CH2)p(CO)q(OCH2CH2)nOH wherein p is an integer selected from 0 or 1; q is an integer selected from 0 or 1; p + q = 1; and n is an integer selected from about 10 to about 100.
US20100189764 Bioactive mesh Surgical meshes include bicomponent fibers and/or microfibers. A bicomponent fiber or microfiber includes a non-absorbable inner core including at least one flexible polymer and an absorbable surface material including at least one rigid polymer. The absorbable surface material has a first stiffness and the non-absorbable inner core has a second stiffness which is lower than the first stiffness. The bicomponent fiber or microfiber surgical mesh is less flexible prior to implantation and more flexible following implantation in tissue. The mesh may be used for the treatment of hernias, vaginal prolapses, and other injuries.
US6982286 Bicarbocyclic hydrazine/hydrazide compounds as inhibitors of semicarbazide-sensitive amine oxidases (SSAO), treat an inflammatory disease or condition, a disease related to carbohydrate metabolism, smooth muscle cell function The present invention is directed to carbocyclic hydrazino compounds that function as inhibitors of copper-containing amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-I (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases. The novel compounds have the general formula: or a pharmaceutically acceptable solvate, hydrate, or salt thereof wherein R1 to R11 are as defined herein.
US7666899 Administering mitglinide or mitglinide calcium hydrate; hypertriglyceridemia; hypercholesterolemia; hyperlipidemia; anticholesteraol agents; antidiabetic agents; glucose intolerance; non-insulin dependendent diabetes; side effect reduction; cardiovascular disorders The present invention provides pharmaceutical compositions for the prevention or treatment of lipid metabolism disorders. The pharmaceutical compositions comprising, as an active ingredient, (2S)-2-benzl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic aid (generic name: mitiglinide) or a pharmaceutically acceptable salt thereof, or a hydrate thereof exert remarkable lipid metabolism improving effect, and are useful for, for example, hyperlipidemia such as hypertriglyceridemia of diabetic patients or the like.
WO2013096055A1 Compounds for inhibiting the interaction of bcl2 with binding partners The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
WO2006019327B1 Deuterium depleted water (ddw) using as adjuvant in cancer therapy for cytostatics toxicity reduction The hereby invention addresses to a new application of Deuterium Depleted Water (DDW), namely, its administering, on a concentration of 60 ppm, as daily diet, to adult healthy outbred Wistar rats produces a distinguished lowering of toxic effects produced by cytostatics (Cyclophosphamide, 5-Flourouracil, Farmarubicine and Vinblastine) when they used in these animals mono-chemotherapy. Also, the 60 ppm DDW administering under similar conditions generates a significant cytostatics toxicity (Cyclophosphamide, 5-Flourouracil, Farmarubicine and Vinblastine) used in polychimiotherapy on pet dogs having different types of cancer. These relevant findings confirm the idea of 60 ppm DDW as a new and efficient adjuvant in cancer chemotherapy on pets and humans.
CN103265558A Hydrobromic acid prasugrel and pharmaceutical composition and application thereof The invention provides hydrobromic acid prasugrel of structural formula (II) and harmaceutical composition and application thereof. The hydrobromic acid prasugrel provided in the invention has good stability, oral absorbability, metabolic activity and platelet aggegation and inhibition effect, low toxicity, therefore the hydrobromic acid prasugrel can be widely used as an anticoagulant drug to prevent or treat diseases caused by thrombus formation or embolism.
CN101074218A Cephalotamannine derivative, its production, its medicinal composition and use A cephalotmannine derivative, composition containing it, its production and use are disclosed. It can be used to prepare drug-resisting medicine in treatment of tumor.
CA2807051A1 Besylate salt of a btk inhibitor The present invention provides a salt form, and compositions thereof, useful as an inhibitor of one or more protein kinases and which exhibits desirable characteristics for the same.
EP1345933B1 Process for making substituted 8-arylquinolinium benzenesulfonate The present invention is directed to a process to synthesize 6-[1-methyl-1-(methylsulfonyl)ethyl]-8-[3(E)-2-[3-methyl-1,2,4-oxadizol-5-yl]-2-[4-(methylsulfonyl)phenyl]ethenyl]phenyl]quinoline and its benzenesulfonic acid salt.
US8084491 Treatments for wound healing The subject invention provides methods of promoting wound healing comprising the administration of a therapeutically effective amount of a composition comprising topiramate. Compositions may administered to a wound site via a salve, ointment, or as a component of a bandage or bioadhesive applied to the site of injury.
US20080025997 Cysteine-rich region of respiratory syncytial virus and methods of use therefor The invention features methods and compositions featuring an RSV Glycoprotein fragment for modulating an immune response in a subject.
CN103394068A Drug for curing acute attack of cervical spondylotic radiculopathy The invention relates to a drug for curing acute attack of cervical spondylotic radiculopathy. The drug is composed of following raw materials in parts by weight: folium turpiniae, semen aesculi, marmor serpentinatum, pomelo flavedo, ligusticum wallichii, garter snake, humifuse euphorbia herb, chinese waxgourd peel, glechoma hedracea, scorpion, dry ginger, cockscomb flower, fructus podophylli, tussilago farfara, hedysarum polybotrys, campsis grandiflora, semen sojae germinatum, chlorite schist, fructus polygoni orientalis, ampelopsis japonica, abalone shell, spina gleditsiae, radix bupleuri, tree peony bark, eucommia, saposhnicovia divaricata, sparganium, chingma abutilon seed, herba lopatheri, caulis marsdeniae tenacissimae, stalactitum, fagopyrum dibotrys, kamuning, bletilla rhizome, longan aril, gorgon fruit, radix psammosilenes, mantis egg-case, tabasheer, fructus gleditsiae sinensis, Chinese starjasmine stem, folium microcotis, artemisia capillaries, pinus tabulaeformis carr, rhizoma atractylodis, rhizoma bolbostemmae, quisqualis, muskmelon seed, lotus leaf and commelina communis L. The drug for curing acute attack of cervical spondylotic radiculopathy has the advantages of simple formula, low price, definite curative effect, and strong adaptability for patients, and is suitable for being applied to the clinic.
WO2008010567A1 Salt or solvate of 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid Disclosed is a novel salt or solvate of 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid. Specifically disclosed are: 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid hydrochloride; calcium 5-methyl-2-(piperazin-1-yl)benzenesulfonate; and a 2,2,2-tetrafluoroethanol-addition product of 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid.
CN101514222A Steroidal compound in Bugula neritina L. and use thereof The invention relates to the field of medical technology and discloses a new steroidal compound which is extracted in marine animal Bugula neritina L. and the application thereof in the preparation of anti-tumor drugs. The general formula of the chemical structure thereof is as follows: the in vitro activity test proves that the steroidal compound has significant anti-tumor activity to three different tumor cells of HepG2, HT-29 and NCI-H460, and the IC50 value is close to or even better than a positive control drug which is vincristine, thereby being capable of being used for preparing the anti-tumor drugs.
WO2014098176A1 Amorphous form of quinoline derivative, and method for producing same The present invention provides an amorphous form of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7- methoxy-6-quinolinecarboxamide.
US20070258986 Targeted Delivery System for Bioactive Agents In accordance with the present invention, compounds, compositions and methods are provided that allow for the administration of a bioactive agent to an organism, including a human or an animal. The present invention can be used to treat or prevent a disease and/or disorder with a bioactive agent, or can be used to safely vaccinate a human or animal against a bioactive agent. The invention can also be used as a method for the delivery of bioactive agents for the treatment or prevention of a disease and/or a disorder, particularly targeted delivery of bioactive agents through the administration of glycoconjugates containing a bioactive agent bound to a targeting compound through a modified saccharide residue.
WO2012069836A3 Biologically active complex and its preparation Biologically active complex and its preparation A biologically active complex comprising either a polypeptide having the sequence of a variant of a naturally occurring protein, wherein said polypeptide is at least partially unfolded as compared to the said naturally occurring protein; or a peptide of up to 50 amino acids, for instance a fragment of the naturally occurring protein or a variant thereof; and a pharmaceutically acceptable salt of a fatty acid or lipid. The complexes of the invention demonstrate a novel mode of action, that gives rise to opportunities for the development of further active agents and screening methods.
EP2612553A1 Compositions and Methods for Prophylaxis and Treatment of Addictions The present invention relates to methods of treating or preventing addiction and relapse use of addictive agents, and treating or preventing addictive or compulsive behaviour and relapse practice of an addictive behaviour or compulsion, by administering a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, alone or in combination with another therapeutic agent, such as, for example, an opioid receptor antagonist or an antidepressant. The present invention also includes pharmaceutical compositions for treating or preventing addiction or relapse that include a PPARγ agonist and one or more other therapeutic agents, as well as unit dosage forms of such pharmaceutical compositions, which contain a dosage effective in treating or preventing addiction or relapse. The methods and compositions of the invention are useful in the treatment or prevention of addiction to any agent, including alcohol, nicotine, marijuana, cocaine, and amphetamines, as well as compulsive and addictive behaviours, including pathological gambling and pathological overeating.
CN102512413A 2-alkyl-benzimidazole-1-acetyl hydrazone and its application The invention discloses 2-alkyl-benzimidazole-1-acetyl hydrazone and its application. The 2-alkyl-benzimidazole-1-acetyl hydrazone compound provided by the invention is 2-methyl-benzimidazole-1-acetyl-(N'-2-hydroxy benzene methylene)hydrazone, 2-methyl-benzimidazole-1-acetyl-(N'-4-hydroxy benzene methylene)hydrazone, 2-methyl-benzimidazole-1-acetyl(N'-4-dimethylamino benzoylate alkene)hydrazone, 2-methyl-benzimidazole-1-acetyl-(N'-3-nitrobenzene methylene)hydrazone, 2-methyl-benzimidazole-1-acetyl-(N'-3,4-oxymethyl methylene)hydrazone, 2-methyl-benzimidazole-1-acetyl-(N'-2-hydroxy-3,5-dibromobenzene methylene)hydrazone, 2-ethyl-benzimidazole-1-acetyl-(N'-4-hydroxy benzene methylene)hydrazone, 2-ethyl-benzimidazole-1-acetyl-(N'-4-dimethylamino benzene methylene)hydrazone or 2-ethyl-benzimidazole-1-acetyl-(N'-3,4-oxymethyl methylene)hydrazone. The above compound can be used as an antagonist for the preparation of a chemotactic factor CXCR4 acceptor and has a good effect.
WO2007137797A1 Gestagen combination and an insulin sensitizer for treating pcos The invention relates to a medicament which, as an active substance combination, contains at least one contraceptively active gestagen as an individual hormone component and at least one insulin sentitizer. Said medicament is particularly suitable for the prophylaxis of or for the therapy of pathological conditions caused by the polycystic ovary syndrome (PCOS).
CN1843353A Use of AR-A014418 in preparing medicine for preventing and treating nerve degenerative diseases The invention relates to the use of AR-AO14418 in preparing medicament for preventing and treating nerve retrogression diseases, wherein the medicament comprises AR-AO14418 and medically acceptable auxiliary materials, wherein the AR-AO14418 can be bonded with the ATP bonding points of the GSK-3 beta, inhibiting GSK-3 beta activity, and preventing hepatocyte nerve.
EP1509516B1 Inhibitors of the gpib -vwf interaction, their preparation and use The present invention relates to compounds of the formula (I); in which R1, R2, A, B, D, E, n, m or o have the meanings indicated below. The compounds of the formula (I) are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb). They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of atherothrombotic diseases.
US20120004282 RNA Interference Mediated Inhibition of the Intercellular Adhesion Molecule 1 (ICAM-1) Gene Expression Using Short Interfering Nucleic Acid (siNA) The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of ICAM-1 gene expression and/or activity, and/or modulate a ICAM-1 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against ICAM-1 gene expression.
US20090186939 Method of Treating Chronic Kidney Disease The present invention discloses pharmaceutical-grade ferric organic compounds having enhanced dissolution rate. These ferric organic compounds, including but are not limited to ferric citrate, are useful for treating chronic kidney disease.
US20060025456 Serotonin reuptake inhibitors; dimethyl-(2-pyridin-3-yl-cyclohex-1-enylmethyl)-amine and the corresponding dihydrochloride; analgesics, anxiety disorders; side effects reduction Saturated and unsaturated heteroarylcycloalkylmethyl-amine compounds corresponding to formula I, processes for their preparation, pharmaceutical formulations comprising these compounds and the use of saturated and unsaturated heteroarylcycloalkylmethyl-amines for the preparation of pharmaceutical formulations. pharmaceutical formulations and related methods of treatment or prophylaxis of certain condition, especially depression and/or pain, are also disclosed.
EP2225230A1 Solid forms of 3-(6-(1-(2,2-difluorobenzoýd¨ý1,3¨dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid The present invention relates to a substantially crystalline and free solid state form of 3-(6-(l-(2,2-difluorobenzo[d][l,3]dioxol-5-yl) cyclopropanecarboxamido)-3- methylPyridin-2-yl)benzoic acid (Form I) of following formula: (I), pharmaceutical compositions thereof, and methods of treatment therewith.
CA2553202A1 Tricyclic benzazepine derivatives as squalene synthase inhibitors used for the treatment of cardiovascular diseases The invention relates to novel tricyclic benzazepine derivatives of formula (I), methods for the production thereof, the use thereof for treating and/or preventing diseases, and the use thereof for producing medicaments used for the treatment and/or prophylaxis of diseases, preferably cardiovascular diseases, particularly dyslipidemia, arteriosclerosis, restenosis, and ischemia.
WO2008084504A2 Pharmaceutical compositions of angiotensin ii receptor blockers The present invention relates to the methods of increasing the bioavailability of Angiotensin II Receptor Blockers (ARBs) by treating it with at least one absorption augmenting agent. In particular, the present invention relates to use of absorption augmenting agents which results in significant increase in the bioavailability as more drug is present in the absorbable form at the absorption site which is in sharp contrast to the currently marketed ARB formulations. In the composition, the ARB may be present in the form of physical blend, solid dispersion, solid solution or complex with absorption augmenting agent. The composition of an ARB with absorption augmenting agent can be incorporated in a tablet, coated tablet, inlay or bilayer tablet or capsule dosage form for immediate release, sustained release, pulsatile release or modified release.
CN101559103A Sterilizing and itching-relieving medical composition The invention discloses a sterilizing and itching-relieving medical composition which comprises the following raw materials of eucalyptus oil, paeonol, carbamide, vitamin E, glycerin, ethanol, glycol polyethylene, antiseptic and essence. The invention has the functions of sterilizing and itching-relieving and is used for solving the problem of skin pruritus.
CA2852917A1 Amine cationic lipids and uses thereof The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).
EP0894000B1 Use for delivering estrogen The present invention relates to methods for the treatment or prevention of osteoporosis and the alleviation of the symptoms of menopause by the administration of an estrogen glycoside or estrogen orthoester glycoside.
CN101100432B Method for synthesizing benzyldimethyl[3-(myristamide)propyl]ammonium chloride Synthesis of benzyl-methyl(3-(myristoyl amino)propyl)ammonia chloride adopts organic acid ester as reactive solvent. It's convenient and non-toxic.
US20110319317 Treatment of sirtuin 1 (sirt1) related diseases by inhibition of natural antisense transcript to sirt1 The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Sirtuin 1 (SIRT1), in particular, by targeting natural antisense polynucleotides of Sirtuin 1 (SIRT1). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of SIRT 1.
US7605154 Substituted Thiazolo [4,5-d]pyrimidines as protein kinase inhibitors The present invention is directed to novel thiazolopyrimidine compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions.
EP1730152B1 Tetrahydroquinoline derivatives and a process for preparing the same A novel compound of the formula (I): wherein R1 is alkoxycarbonyl or the like, R2 is alkyl or the like; R3 is hydrogen or the like; R4 is alkylene or the like; R5 is optionally substituted heterocyclic group; R6, R7, R8 and R9 are independently hydrogen; alkyl, alkoxy, or the like; R10 is optionally substituted aromatic ring, or the like; or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP).
US20120046302 Methods of treating cns disorders The present invention relates to methods of treating various CNS disorders, e.g., mania, bipolar disorder and schizophrenia, by administering NMDA receptor antagonists, alone or in combination with dopamine receptor antagonists.
CN102816150A Indole with bacteriostatic activity and derivatives thereof-triazole compounds, and preparation method thereof The invention discloses an indole with bacteriostatic activity and derivatives thereof-triazole compounds, and a preparation method thereof. The technical scheme is as follows: the structural general formula of the indole with bacteriostatic activity and derivatives thereof-triazole compounds is disclosed in the specification, wherein X1 can be halogen atom, alkoxy group, alkyl group, haloalkyl group, aldehyde group, carboxy group, sulfonic group, OH, NH2, NO2 or SH; X2 can be Ar, alkyl group, cycloalkyl group or R1COOR2; and R1 and R2 can be respectively alkyl group or cycloalkyl group. The invention also discloses a preparation method and application of the compounds. In the invention, water is used as a solvent, CuCl2/Zn is used as a catalyst, and stirring is carried out at room temperature to synthesize the indole with bacteriostatic activity and derivatives thereof-triazole compounds. The reaction process has the advantages of high yield, high selectivity and environmental protection. The bacteriostatic activity test proves that the compounds have great potential in the fields of medicine, pesticides, fine chemical engineering and the like.
US20110009318 Transdermal Compositions and Methods for Treatment of Fibromyalgia and Chronic Fatigue Syndrome Compositions and methods for alleviating the symptoms associated with chronic fatigue syndrome and fibromyalgia syndrome are provided. The compositions are based on use of a transdermal gel formulation delivery system for androgens, either alone or in combination with other hormones.
US20050191690 Membrane proteins for identifying modulators for prevention and treatment of infection, cell proliferative, neurological, cardiovascular, gastrointestinal, autoimmune/inflammatory and metabolic disorders The invention provides human G-protein coupled receptors (GCREC) and polynucleotides which identify and encode GCREC. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating, or preventing disorders associated with aberrant expression of GCREC.
CN102727512A Optimized adult first-line AIDS antiviral therapy program The invention provides an optimized adult first-line AIDS (Acquired Immune Deficiency Syndrome) antiviral therapy program. Concretely, the therapy program of the invention includes (a) a first stage: employing the stavudine-containing (D4T) program to treat for a period of time (such as 4-12 months); and (b) a second stage: replacing stavudine with zidovudine (AZT) for treatment. The therapy program of the invention not only gets a good therapeutic effect, but also can reduce the toxic and side effects of D4T and AZT, and is an equivalent and relatively safe first-line therapy program.
WO2009122435A3 Simultaneous preparation of a mixture of 3- acetoxy-17-acetamido-16-formyl-androst-5,17-diene and 3- acetoxy-2'-chloro-5-androsteno[17,16-b]pyridine The present invention relates to preparation and biological evaluation of 3-acetoxy-17- acetamido-16-formyl-androst-5,17-diene (4) and 3-acetoxy2'-chloro-5-androsteno [17,16- b]pyridine (5) as gastric proton pump inhibitor and their comparison to that of omeprazole, a clinically employed anti-gastric ulcer drug. Compound (4) exhibited dose dependent inhibition of histamine-stimulated acid secretion in gastric parietal cell with an IC50 value comparable to cimetidine. No mortality or behavioral abnormality of Swiss albino mice was observed under single-dose level of 1g/Kg body weight of compound (4). Compound (4) further exhibited excellent anti ulcer activity in vivo against indomethacin induced ulcer.
EP0906108B1 Endothelin antagonists for treating heart failure The present invention is concerned with prevention and/or treatment of heart failure with compounds that are endothelin antagonists.
CN1965948A Pharmaceutical composition not only capable of treating acne but also having face-beautifying function The invention discloses a pharmaceutical composition having beauty treatment effect for treating acne, which comprises rhubarb horsetails, root of red rooted saliva, dahurian angelica root, astragalus root, citron fruit, red halloysite, licorice root, borneo camphor and momordica seed. The composition is effective in treating acne, and has the advantages of low cost, short course of treatment, higher curing rate, and low recurrence rate.
WO2009003255A1 Pharmaceutical compositions comprising semicarbazones and thiosemicar-bazones and method for treating inflammatory, painful and febrile conditions and preventing signs and symptoms The present patent application refers to pharmaceutical compositions comprising at least a semicarbazone or a thiosemicarbazone, or a pharmaceutically acceptable salt, hydrated or solvated thereof, for the treatment of inflammatory, febrile and painful inflammatory conditions, inflammatory edema and peripheral or central neurophatic painful conditions or prevention of signs and symptoms of inflammation. Claim also pharmaceutical compositions comprising at least a semicarbazone, or a thiosemicarbazone, or a pharmaceutically acceptable salt, hydrated or solvated thereof and a therapeutically effective amount of these compounds, mixed or included in a pharmaceutically acceptable carrier or excipient or a thiosemicarbazone is provided as sustained or controlled release systems for human and veterinary use in solutions or in the solid state.
CA2346539C Compositions and methods for enhancing receptor-mediated cellular internalization Compositions and methods for improving cellular internalization of one or more compounds are disclosed. The compositions include a compound to be delivered and a biocompatible viscous material, such as a hydrogel, lipogel, or highly viscous sol. The compositions also include, or are administered in conjunction with, an enhancer in an amount effective to maximize expression of or binding to receptors and enhance RME of the compound into the cells. This leads to high transport rates of compounds to be delivered across cell membranes, facilitating more efficient delivery of drugs and diagnostic agents. Compositions are applied topically orally, nasally, vaginally, rectally, and ocularly. The enhancer is administered with the composition or separately, either systemically or preferably locally. The compound to be delivered can also be the enhancer.
US20110052665 Haemostatic material The present invention relates to a haemostatic material comprising a carrier layer and a material for wound contact comprising at least one haemostat in particulate, granular, powder, flake or short fibrous form. Such a haemostatic material is useful, for example, in reducing or stopping bleeding of a physiological target site in a person or animal, and can also be used to stem bleeding during medical procedures.
CN102552321A Hemostatic suppository and preparation method thereof The invention relates to a hemostatic suppository and a preparation method thereof. The hemostatic suppository contains the following components in percentage by weight: 9% to 15% of sodium humate, 0.9% to 1.1% of borneol and fat-soluble matrices. The hemostatic suppository has hemostatic and analgesic effects and is convenient to administer, safe and painless.
EP1399468B1 2-((n-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl)-amino)-alkylboronic acid derivatives The present invention relates to compounds of formula (I) their synthesis and pharmaceutical compositions thereof for the therapeutic treatment of a proliferative diseases in warm-blooded animals, including humans.
US7531567 effector ambroxole with ACE inhibitors; treatment of a disturbance of the thiol-disulfide status in kidney replacement therapy The invention relates to the use of the combination of n-lipoic acid and effectors of the glutathione metabolism for the treatment of disturbances of the cellular thiol status and accompanying disorders in kidney replacement therapy.
EP2507374A2 Novel therapeutic rna interference technology targeted to the pdx-1 oncogene in pdx-1 expressing neuroendocrine tumors A bifunctional shRNA-based composition and methods for knocking down the expression of the PDX-I oncogene in target cells is described herein. The invention also provides methods to deliver the shRNA-containing expression vectors to target tissues overexpressing the PDX-I oncogene.
US20100087360 Heterocycle-substituted benzimidazole derivative A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein X1 to X4 independently represent a carbon atom or the like; the ring A represents a 5- to 6-membered heteroaryl having 1 to 4 heteroatoms independently selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom; X5 represents an oxygen atom or the like; X represents a carbon atom or the like; Het represents a 5- or 6-membered aliphatic heterocycle; R1 represents an aryl or the like; R2 represents a formyl group or the like; and R3 represents a —C1-6 alkyl or the like. The compound or salt has a glucokinase activation effect and is useful as a therapeutic agent for diabetes.
CN101257906A Stable solid formulation of sertindole The present invention relates to a pharmaceutical composition comprising sertindole and a protective agent absorbing radiation with a wavelength below 400 nm. The present invention also relates to the use of sertindole for the preparation of a pharmaceutical composition comprising sertindole and a coating layer comprising said protective agent, such as ironoxide, for the treatment of schizophrenia.
CN103328474A Salts and crystalline forms of an apoptosis-inducing agent Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}- sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
US20110201675 ON01910.Na ENHANCES CHEMOTHERAPEUTIC AGENT ACTIVITY IN DRUG-RESISTANT TUMORS The invention includes compositions and methods of treatment of cancers susceptible to treatment with nucleotide analog chemotherapeutic agent, including cancers in which nucleotide analog resistant tumors have developed, including identifying a subject having cancer susceptible to treatment with a nucleotide analog chemotherapeutic agent and a mitotic disruptor/polo-like kinase (Plk) pathway inhibitor to a subject; and monitoring the subject for a reduction or stabilization of at least one sign or symptom of cancer.
EP1883636A1 Substituted piperidine antagonist of hi receptor to be used for the treatment of rhinitis The present invention relates to the compound, (I) and salts thereof, processes for its preparation, to compositions containing it and to its use in the treatment of various disorders, such as allergic rhinitis.
WO2013105065A1 Fused piperidines as ip receptor agonists for the treatment of pah and related disorders The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed.
CN1827627A Novel acyclic nucleoside phosphonic acid and its ester derivatives and pharmaceutical use thereof Disclosed is a non-cyclic nucleotide phosphonic acid represented by formula (I) and its ester derivative, its non-toxic pharmaceutically acceptable salts, or their hydrates or solvates, wherein R1 represents C1-C6 alkyl, X represents NH or S, R2 represents hydrogen, C1-C3 alkyl or halogen substituted alkoxy, C1-C3 alkyl or halogen substituted alkyl, halogen, R3 represents H, C1-C3 alkyl, C1-C3 hydroxyl substituted alkyl or C1-C3 alkyl substituted by more than one halogen atoms, R4 and R5 represent H, C1-C22 alkyl, phenyl, acylorxy or alkyl substituted by more than one halogen atoms. Z represents C or N.
WO2004005313A3 Hybrid molecules of macrolides with steroid/non-steroid anti-inflammatory, antineoplastic and antiviral active molecules The present invention relates (a) to new compounds represented by Formula I wherein M represents a macrocode subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, V represents and ant-inflammatory steroid or nonsteroid subunit, or an antineoplastic or antiviral subunit and L represents a linking group covalently linking M and V; (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory/neoplastic/viral diseases and conditions in humans and animals.
US20070219159 Cyclodextrin compositions and methods of treating viral infections The present invention provides methods and therapeutic compositions for treating viral infections.
US20100298438 Gene expression profiling of parkinson's disease The present invention identifies the changes in gene expression associated with Parkinson's Disease by examining multiregional gene expression from normal brain and brain of Parkinson's Disease. The present also identifies the changes in gene expression associated with Parkinson's Disease by examining the expression of genes from normal blood and from the blood of patients with Parkinson's Disease. In another aspect, the present invention identifies expression profiles which serve as useful diagnostic markers as well as markers that can be used to monitor disease states, disease progression, drug toxicity, drug efficacy and drug metabolism.
WO2009106752A3 Derivatives of 2-heteroaroyl-imidazol[1,2-a]pyridine, preparation thereof and therapeutic application thereof The invention relates to compounds of the formula (I) in which: X is a benzodioxole group, a heteroaromatic group bonded by a carbon atom; R2 is a hydrogen atom, a halogen atom, a (C1-C6) alkyl group, a (C1-C6) alkoxy group, a (C1-C6) alkylthio group, a (C2-C6) alkenyl group, a (C2-C6) alkynyl group, a -CO-R5 group, a CO-NR6R7 group, a -CO-O-R8 group, a -NR9-CO-R10 group, a -NR11R12 group, a cyano group, a phenyl group, a heterocyclic group; R1 is a hydrogen atom, a halogen, a (C1-C6) alkoxy group, a (C1-C6) alkyl group, hydroxy or amino; R3 is a hydrogen atom, , a (C1-C6) alkyl group, a halogen atom of a hydroxy group; R4 is a hydrogen atom or a halogen atom; said compounds being in the state of a base or an addition salt to an acid. The invention can be used in therapeutics.
US20120053243 Parakeratosis inhibitor and skin preparation for external use To provide a parakeratosis inhibitor, pore reducing agent and skin roughness preventing/ameliorating agent that exhibit capabilities of parakeratosis inhibition, pore reduction, skin roughness prevention/amelioration, etc., and further provide a skin preparation for external use having these capabilities. There are provide a parakeratosis inhibitor and a pore reducing agent each comprising at least one compound selected from the group consisting of a glycine derivative, an aminodicarboxylic acid derivative, an acylaminodicarboxylic acid derivative, a pyrrolidinecarboxylic acid derivative, a piperidinecarboxylic acid derivative, a hexamethyleneiminecarboxylic acid, a beta-alanine derivative and salts of these derivatives. Further, there are provided a parakeratosis inhibitor, a pore reducing agent and a skin roughness preventing/ameliorating agent each comprising at least one compound selected from the group consisting of specified glycine derivatives and salts thereof and specified aminosulfuric acid derivatives and salts thereof. Still further, there are provided skin preparations for external use comprising these compounds.
CN101305999A Use of 2-alkyl substituted 4,6-diamino-1,3-5-triazine derivate The invention provides the application of 2-alkyl substitution4, 6-diamino-1, 3, 5-triazine derivatives to the preparation of anti-neoplastic drugs. Research shows that the 2-alkyl substitution4, 6-diamino-1, 3, 5-triazine derivatives have the proliferation inhibiting action on multiple cancer cell strains, more particularly have obvious inhibition action on multiple tumor cell strains such as human lung cancer A549 cells, human leukemia K562 cells, human prostatic cancer PC-3 cells, human ovarian cancer HO8910 cells, human breast cancer MCF-7 cells, etc., and the antitumor spectra is wider.
US20120009264 Drug carrier for treating of gastrointestinal ulcer A drug carrier for treating of gastrointestinal ulcer comprises a microspheroid having a substrate and a plurality of particles distributed over and covered by the substrate, wherein the substrate is alginate and the plurality of particles is a drug for treating of gastrointestinal ulcer; and a coat covering up the surface of the microspheroid, which contains chitosan.
CA2803689A1 Method for treating ophthalmic diseases using kinase inhibitor compounds in prodrug forms This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula (I) to the eyes of the patient in need of.
CN102228555A Medicinal liquid for treating burns and scalds The invention discloses a medicinal liquid for treating burns and scalds, which is characterized by being prepared by the following steps of: frying Polygonum cuspidatum, burnet, lithospermum, phellodendron amurense, rhubarb and Fructus Gardeniae in high-temperature sesame oil till all the medicinal herbs become yellow; removing dregs and keeping decoction; cooling; putting borneol and mint into filtrate; and subpackaging. The medicinal liquid has the effects of removing heat, cooling blood, detoxifying, eliminating swelling, stopping pains, removing carrion and regenerating new muscles and can stop pains and prevent infections of burns and scalds caused by different reasons; and compared with moist burn treating ointment and Jingwanhong ointment, the medicinal liquid has a better therapeutic effect than a control group, and clinical observations prove that the effectiveness of the medicinal liquid is 100 percent.
WO2009105278A3 Nanoparticle targeted drug delivery to the lungs using extra-testicular sertoli cells A method of delivering a compound of interest to the lungs of a subject by the intravenous injection of Sertoli cells loaded with a plurality of chitosan nanoparticles coupled with the compound of interest is provided. Testis-derived rat Sertoli cells were pre-loaded with chitosan nanoparticles coupled with or without the drug curcumin, pre-labeled with a fluorescent cell marker and then injected intravenously into the control or asthmatic mouse model host. Intact pre-loaded, pre-labeled Sertoli cells were present in the lungs at 15 minutes post-injection, appeared entrapped in the pulmonary pre-capillary vascular bed around alveolar sacs but were not present one hour post-injection although Sertoli cell label and cellular debris was. Most of the of the injected nanoparticle load (70%) and curcumin load (80%) was present in the lungs 15 minutes post-injection, and remained at 70% and 80%, respectively, one hour post-injection.
CN102675282A Substitutive quinoline compound and application method and uses thereof The invention provides substitutive quinoline compound, pharmaceutically acceptable salts of the substitutive quinoline compound, and pharmaceutical preparations of the substitutive quinoline compound. The substitutive quinoline compound, the pharmaceutically acceptable salts and the pharmaceutical preparations are used to adjust activity of protein kinase and intercellular or intracellular signal response. The invention further relates to drug combinations of the substitutive quinoline compound, and a method of using the drug combinations to treat mammals, especially human with highly proliferative diseases.
US20120207758 CD22 Exon 12 Deletion Mutants Provided herein are CD22ΔE12 polynucleotides and polypeptides, as well as diagnostic compositions and methods for identifying patients suffering from B-cell disorders such as leukemias, and particularly for identifying aggressive disease. Use of the disclosed association of specific CD22ΔE12 gene and polypeptide mutants with specific disease and prognosis also provides new targeted therapies for the associated disorders.
CN101390991A Medicine for treating coryza, chronic nasal sinusitis The invention relates to a medicine for curing coryza and chronic nasosinusitis, which is characterized in that the medicine is composed of following raw materials by weight ratio: 80 to 120 parts of camellia oil, 8 to 12 parts of gypsum and 8 to 12 parts of borneol. The medicine has the advantages of effectively restraining and killing pathogen, reducing swelling, alleviating pain, stanching the bleeding, nourishing skin and generating muscle, improving the inner environment in nasal cavity and paranasal sinuses, improving the ventilation function of the nasal cavity and effectively curing coryza and chronic nasosinusitis, with low cost and immediate curative effect as well as without easy recrudescence.
DE102010055771A1 Composition useful as a medicament for therapeutic, prophylactic, cosmetic or health-promoting functions in e.g. humans comprises chlorite and polyvalent alcohol in aqueous or alcoholic-aqueous chlorine dioxide-containing solution Composition comprises at least one chlorite and a polyvalent alcohol in aqueous or alcoholic-aqueous chlorine dioxide-containing solution without other chlorine oxide compounds, chlorates and oxidants, preferably peroxides. The composition has a pH value of >= 4. Independent claims are also included for: (1) a solid material composition for preparing the composition by dissolving the solid material composition in water and/or alcohol; and (2) an agent for internal or external application for therapeutic, prophylactic, cosmetic or health-promoting functions in humans and animals, comprising the composition or the solid material composition. - ACTIVITY : Antibacterial. No biological data given. - MECHANISM OF ACTION : None given.
WO2009109836A1 Oral galenic formulation including ketorolac and b-complex vitamins, in which vitamin b6 is in an outer layer separated from the rest of the active principles The invention relates to a solid oral pharmaceutical composition combining ketorolac and B-complex consisting of inter alia thiamin, pyridoxine and cyanocobalamin (vitamins B1, B6 and B12 respectively) and/or the pharmaceutically acceptable salts thereof, as well as pharmaceutically acceptable excipients and/or vehicles. The invention also relates to the method for producing the composition and to the use of said composition having a synergistic therapeutic activity, indicated for the treatment of moderate to severe pain or neuralgias in different locations.
WO2014033366A1 Pharmaceutical compositions of anisomelic acid and the use thereof A pharmaceutical composition for anti-viral cancer treatment in mammals,comprising a therapeutically effective amount of Anisomelic acid or salts thereof. The pharmaceutical composition may comprise Anisomelic acid or salt thereof in an oil-in-water emulsion, for example in an isotropic mixture of at least one oil and at least one surfactant or, alternatively, in a hydrophilic solvent and a co-solvents or surfactant or a combination thereof.A method of treating or preventing of cancer in a mammal, wherein the p53 pathway is deregulated by viral oncoproteins, is also provided.
EP2666774A1 Beta-lactamase Inhibitors Substituted bicyclic beta-lactams of Formula I: are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
EP2440216A1 Use of a composition for the treatment of mucositis The present invention relates to a composition comprising an ionic complex of chitosan and a negatively charged polysaccharide, selected from the group consisting of heparin, heparan sulfate and dextran sulfate, for use in the treatment of mucositis in a mammalian subject, to a method of preventing or treating mucositis ina mammalian subject, by applying topically a compositioncomprising an ionic complex of chitosan and a negatively charged polysaccharide, selected from the group consisting of heparin, heparan sulfate and dextran sulfate. The present invention further relates to a pharmaceutical composition for topical administration comprising an ionic complex of chitosan and heparin.
US20100317695 Gel composition for treating mycosis The present invention aims to provide a gel composition for mycosis treatment, which ensures good absorption and permeation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol into a target site (skin and nail). The present invention also aims to provide a gel composition for mycosis treatment, which is excellent in stability of this drug. It is a gel composition for mycosis treatment, which comprises (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol or an acid addition salt thereof, a lower alcohol, a polyhydric alcohol and a gel-forming polymer. The gel composition of the present invention is excellent in permeation of KP-103 into a target site and also excellent in permeation into the nail. Thus, the gel composition of the present invention allows the drug to be directly and rapidly absorbed and permeated into a target site in a constant manner, and thereby produces an excellent effect in mycosis treatment, particularly onychomycosis treatment.
WO2013055985A1 Combinatorial compositions and methods of treating hemoglobinopathies Provided herein are compositions and methods for increasing fetal hemoglobin expression (HbF) for the treatment and/or amelioration of the symptoms of a hemoglobinpathy in a mammal. The compositions comprise a combination of one or more inhibitors of BCL11A expression or activity with epigenetic modifers, such as inhibitors of DNA methylation and/or one or more inhibitors of histone deacetylases.
EP1425000B1 Use of polysubstituted indan-1-ol systems for producing drugs used in the prophylaxis or treatment of obesity The invention relates to the use of polysubstituted indan-1-ol systems and the physiologically acceptable salts and physiologically functional derivatives thereof for producing drugs used in the prophylaxis or treatment of obesity. The invention relates to the use of the compounds of formula (I), wherein the groups are defined as indicated, and to the physiologically acceptable salts and physiologically functional derivatives thereof for producing a drug used in the prophylaxis or treatment of obesity.
US7037920 Substituted tricyclic himbacine derivatives that are useful as thrombin receptor antagonists Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salts thereof, wherein: n1 and n2 are independently 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is alkyl or optionally substituted alkenyl; R22 is —COR23 or a carboxy, sulfinyl, sulfonyl, sulfonamide or amino acid derivative; R23 is haloalkyl; alkenyl; haloalkenyl; alkynyl; optionally substituted cycloalkyl; cycloalkyl-alkyl; aryl; arylalkyl; heteroaryl; heterocycloalkyl; or —COOH and/or —SO3H substituted alkyl; R1, R2, R3, R9, R10 and R11 are as defined in the specification; are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds.
US20110077232 Compositions comprising atorvastatin 4-(nitrooxy) butyl ester and a hypolipidemic drug The present invention relates to compositions comprising atorvastatin 4-(nitrooxy) butyl ester and a hypolipidemic, in particular ezetimibe and fenofibrate. The invention discloses also their use as cholesterol-reducing drugs, as drugs having immunosuppressive properties, antioxidant, antithrombotic and anti-inflammatory activity, effects on endothelial function, and for treating and/or preventing acute coronary syndromes, stroke, atherosclerosis, neurodegenerative disorders, such as Alzheimer's and Parkinson's disease as well as autoimmune diseases, such as multiple sclerosis.
US7304056 N-(3-tetrahydrobenzodiazepinonyl)succamides: 2R,3S)N1-[1,3,4,5-tetrahydro-1-(3-phenoxybenzyl)-2-oxo-5-(phenyl)-2H-1,5-benzodiazepin-3-yl]-2-(2-methylpropyl)-3-(propyl)-butanediamide; inhibit production of A beta -peptide, preventing neurological amyloid deposits; Alzheimer's disease This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
US20070185094 Novel 3-substitued-1,4-benzodiazepines The present invention relates to compounds of formula (I). The invention also relates to methods for preparing the compounds and their uses as CCK receptor ligands and CCK antagonists.
US20070293553 Diphenylurea Derivatives Useful As Potassium Channel Activators The present invention relates to the medical use of a certain group of diphenyl urea derivatives as potassium channel blockers for treating cardiovascular diseases, an obstructive or inflammatory airway disease, urinary incontinence, psychosis, epilepsy or pain, or for facilitating the blood-brain barrier permeability for other therapeutic substances. In other aspects the invention relates to the use of these compounds in a method of therapy.
US20060223803 Process for resolving aimines that are useful for the treatment of disorders associated with insulin resistance syndrome The present invention is directed towards a process for resolving a racemic amino compound derived from dihydro-1,3,5-triazines. The invention is also directed towards the enantiomers of amino derivatives of dihydro-1,3,5-triazines and to their use for the preparation of medicaments, in particular for the treatment of diabetes and malaria.
CN101347464B Health products capable of reducing blood sugar and method of preparing the same The invention provides a health care product for decreasing blood sugar and a preparation method thereof. The product produces genetic characteristics variation of monascus strains in the space environment and cultivates the bacteria with stable genetic characteristics by sifting on the earth. The bacteria stores in the ordinary microorganism center of China Committee for Culture Collection of Microorganisms and the serial number is CGMCC No.2614. The bacteria is manufactured to red yeast rice through seed culture, solid fermentation, baking and grinding and then the red yeast rice is mixed with propolis, chromium picolinate, pearl shell powder and western ginseng powder for preparation. The health care product prepared by the invention can effectively decrease blood sugar with small toxicity and side effect and has obvious effect on prevention and adjuvant therapy of diabetes.
WO2008127138A1 Composition for decelerating the ageing in the organism and for extending the life time thereof and the use of said composition The invention relates to pharmacology, medicine and gerontology, in particular to a class of chemical structures (1) which can be used in compositions, in the form of geroprotectors, for extending the life time, decelerating, stopping or for reversing the process of the entirety of the organism's dysfunctions causing the mammal ageing and for preventing and treating particular senile diseases.
WO2012126084A1 Hsp-90 binding compounds, compositions thereof, and their use iν the treatment and prevention of fungal infections The invention relates to therapeutic compounds that bind to HSP90. The compounds disclosed herein bind HSP90 and alter the chaperoning capability of HSP90 proteins. The invention also relates to pharmaceutical compositions comprising these compounds, and methods of treating or preventing fungal infections.
CN1969861A Sustained release system of clozapine solid liposome microparticle The invention discloses a clozapine solid liposome microparticle control slow-release system, which is characterized by the following: adopting high-fusing point and biological compatible solid liposome as carrier material such as fatty acid ester, fatty acid, fatty alcohol or their two composition; making surface activator or macromolecule as stabilizer such as lecithin, poloxamer series, polysorbate series, cholate and so on.
CN101675977A Formula comprising black alum for treating hepatopathy A formula for treating hepatopathy comprises, based on the weight percentage, 20 to 35% of black alum, 10 to 15% of walnut, 20 to 35% of flour, 10 to 15% of charred human hair, and 20 to 35 % of brownsugar. The walnut is coated by yellow mud and stewed for preserving the nature, the charred human hair is baked into a charcoal by using a tile, the flour is fried with a spoon until the flour is yellow, the black alum, the walnut, the charred human hair and the flour are mixed into a powder, the powder and the brown sugar are smelt to form a pill, one pill is taken each time, and pills are takenbefore meals in three times every day.
US20060228407 Enhanced delivery via serpin enzyme complex receptor Serpin enzyme complex receptors are used as targets for therapeutic drugs in the lungs and brain tissue. any lung or brain disease and any therapeutic drug can be targeted to the lung or brain by use of ligands which specifically bind to the receptors. Complexes for delivery may include proteins, pharmacological agents, or nucleic acids, as well as carrier molecules, and ligands for the receptors. The ligands can be coupled directly to the therapeutic agent or to a carrier molecule which binds to the therapeutic agent.
US7244706 For therapy of bacterial infections The present invention provides a therapeutic method for treating or preventing a disease resulting from a microbial infection in an individual using an antimicrobial polypeptide. The present invention also provides a method of potentiating the therapeutic action of an antimicrobial drug in a patient. Further provided in the present invention are methods for neutralizing circulating endotoxin in a patient by administering the endotoxin-neutralizing polypeptide or functional variant thereof of the present invention to the patient.
US7217726 Oxazolidinon-3-ylphenyl -piperazine, -imidazolidine, and -diazepine derivatives, e.g., S)-N-[3-[3-Fluoro-4-[4-(5-nitrofuran-2-ylthiocarbonyl)piperazin-1-yl]phenyl]-2-oxooxazolidin-5-ylmethyl]thioacetamide; treating bacterial infections, particularly those that are antibiotic resistant The present invention provides novel compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel oxazolidinone derivatives of the general formula (I)
US20120220619 Rapamycin Derivative or an Impdh Inhibitor for Treating Polycystic Kidney Disease A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5′-monophosphate dehydrogenase inhibitor or a rapamycin derivative.
CN101011402A Compound sulfadimidine sodium injection and its preparation method The invention relates to a method for preparing composite sulfadimidine sodium injection, formed by 5-20 deals of sulfadimidine sodium, 5-20 deals of bosporon sodium, 1-3 deals of enoxacin, and 0.5-3 deals of TMP. And the preparation comprises that weighting the materials; dissolving sulfadimidine sodium, bosporon sodium, and enoxacin into water, adding some assisting solvent, mixing until transparent, adding TMP, mixing, combing the solutions, mixing uniformly, adjusting the pH value, adding active carbon, mixing and absorbing for 15-20min, adding injection water to 1000 deals. The inventive agent can be used to treat the general infection of pig with significant effect.
WO2007128987A2 Therapy targeting cathepsin s The invention relates to a method of inhibiting chemotherapy induced upregulation of Cathepsin S on the surface of tumour cells, the method comprising the administration of a Cathepsin S inhibitor to said cells. Also provided is a therapy comprising an anti Cathepsin S antibody, in particular an anti-Cathepsin S antibody which does not inhibit the proteolytic effect of Cathepsin S but nevertheless inhibits angiogenesis and a combination treatment comprising a Cathepsin S inhibitor and a therapeutic agent.
CN103709135A Xanthone derivative and preparation method and application thereof The invention discloses a compound shown in a general formula (I) or a pharmaceutically acceptable salt thereof, wherein n is a positive integer of 2-6; R is halogen, -NR1R2, nafoxidine, piperidine, morphine-linda and the like. The xanthone derivative disclosed by the invention has good anti-tumor activity, and can be applied to treatment of diseases such as a gastric cancer, a lung cancer, a nasopharynx cancer, lung adenocarcinoma, a liver cancer, a colon cancer, a breast cancer and the like.
WO2007094413A1 Medicinal composition for transdermal administration It is intended to provide a medicinal composition for transdermal administration which has a favorable texture in using and exerts an excellent therapeutic effect on skin ulcer such as bedsores. A hydrogel type composition, which is prepared by combining (i) an aqueous hypochlorous acid solution with (ii) native gellan gum, is used as a medicinal composition for transdermal administration.
EP2252287A1 Use of inhibitor of beta-lactamases and its combination with beta-lactam antibiotics The present invention relates to a pharmaceutical composition with broad-spectrum of activity against class A, class C and D enzymes comprising an antibiotic and a pharmaceutically effective amount of a compound of Formula (I), compounds of Formula (I), the use of a therapeutically effective amount of one or more compounds of Formula (I) as a broad-spectrum beta-lactamase inhibitor and the use of such a pharmaceutical composition for the treatment of an infection in humans or animals caused by bacteria.
CN102218142A Method for enhancing bacteriostatic effect of deep fungal-infection resistant antifungal medicament The invention belongs to the field of antifungal medicaments, and particularly relates to a method for enhancing bacteriostatic effect of an antifungal medicament. The method is implemented by combinedly treating fungus by a method of blocking a calcium ion signal system and a medicament for blocking biosynthesis of fungal ergosterol, wherein the method of blocking the calcium ion signal system can implement removal by a blocking agent for transmitting calcium signals in the calcium ion signal system as well as an important protein inhibitor or gene. The calcium signal system blocking agent and fungal ergosterol are synthesized into the blocking agent, the secondary bacteriostatic concentration of azole medicament and a certain concentration of calcium ion signal system blocking agent without toxic action on fungus are mixed, the mixture is added into a fungal culture medium, and fungal spores are dropped on the culture medium mixed with the medicament. The result proves that the diameter of the colony on a flat plate which is administrated by the two medicaments is obviously reduced, which indicates that the two bacteriostatic effect of the combined administration of the two medicaments is better.
CN103275138A Carbon 16 zero double bond diacetylation lactone sophorolipid and application thereof The invention discloses a compound carbon 16 zero double bond diacetylation lactone sophorolipid and an application thereof in preparing medicine for preventing and curing liver cancer, lung cancer, esophagus cancer, stomach cancer and breast cancer. Tests show that the chemical compound has strong inhibition effect to HepG cell2 of liver cancer, A-549 cell of lung cancer, SGC7901 cell of stomach cancer, KYSE109 cell of esophagus cancer and MDA-MB-435 cell of breast cancer for people when the concentration is 50 mg/kg, provides foundation and approach for antineoplastic drug which resists various tumors, has less toxic side effects and obvious effects, and has vital meaning.
WO2008031439A3 Treatment of insulin resistance or diseases associated with insulin resistance with bicyclo [ 3.2. i ]octans such as steviol and isosteviol The present invention relates to the use of a substance with the core structure of formula (I), or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the manufacture of a composition for the treatment of insulin resistance or diseases associated with insulin resistance, preferably in human subject in a daily dosage in a range of from about 5 mg to about 1500 mg. The invention furthermore relates to a method of treating insulin resistance or diseases associated with insulin resistance in a mammal, said method comprises administering to said mamma, preferably a human subject, a substance with the core structure of formula (I), preferably in a daily dosage in a range from about 5 mg to about 1500 mg. The substance is preferably isosteviol or steviol, or pharmaceutically acceptable salts, solvates or prodrugs thereof. Examples of diseases associated with insulin resistance are e.g. type 2 diabetes mellitus, insulin resistance syndrome, impaired glucose tolerance, the metabolic syndrome, hyperglycemia, hyperinsulinemia, arteriosclerosis, hypercholesterolemia, hypertriglyceridemia, hyperlipidemia, dyslipidemia, obesity, central obesity, polycystic ovarian syndrome, hypercoagulability, hypertension, microalbuminuria, or any combinations thereof.
US7196067 Which is complementary to a portion of the nucleic acid sequence encoding IGFBP-2 and which reduces the amount of IGFBP-2 in the treated cells; gene expression inhibition Compositions and a method are provided for the treatment of prostate and other endocrine tumors in mammals, including humans, by administration of an antisense oligodeoxynucleotide (ODN) which is complementary to a portion of the gene encoding IGFBP-2. Using the Shionogi tumor model in vitro and in vivo, the administration of such an ODN was shown to reduce proliferation of tumor cells, and also to delay the progression to androgen independence. Thus, treatment of prostate and other hormone-regulated cancer in mammals, including humans, and delay of the progression of prostate tumors to androgen independence is accomplished by administering to the mammal a therapeutically effective amount of an antisense oligodeoxynucleotide which is complementary to a portion of the nucleic acid sequence encoding IGFBP-2 and which reduces the amount of IGFBP-2 in the treated cells.
US20050123533 Prodrugs activated by targeted catalytic proteins Disclosed and claimed are prodrugs activated by catalytic proteins, such as enzymes and catalytic antibodies. The invention comprehends such prodrugs, as well as haptens, to elicit catalytic antibodies to activate the prodrugs. The prodrugs are useful as cytotoxic chemotherapeutic agents; e.g., as antitumor agents.
US7196090 Nitrogen compounds such as 1-cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-(4-dimethylamino -butylamino)-1H-pyrimido (4,5-d)pyrimidin-2-one used as cyclin-dependent and tyrosine kinase enzymes inhibitors; anticarcinogenic agents This invention provides phenyl-substituted pyrimidopyrimidines, dihydropyrimido-pyrimidines, pyridopyrimidines, naphthyridines, and pyridopyrazines of the general formula: that inhibit cyclin-dependent kinase and tyrosine kinase enzymes, methods and intermediate compounds for their synthesis, as well as pharmaceutical compositions and methods for their use in treating, inhibiting or preventing maladies associated with cell proliferative disorders, including angiogenesis, atherosclerosis, restenosis, and cancer.
EP1180991B1 Gambogic acid derivatives as activators of caspases and inducers of apoptosis The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by general Formulae (I-III) wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formulae (I-III) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled cell growth and spread of abnormal cells occurs.
CN1813777A Medicine for treating diabetes retina disease The present invention relates to a natural medicine extract composition for curing diabetic retinopathy and its application. It is formed from baicalin and notoginseng total saponin, and can be made into dripping pills and dispersing tablet. In said medicine composition the puerarin, sodium ferulate, hypericin and curcumin also can be added, and can be used for curing the diseases of diabetic renopathy, cerebral apoplexy, vascular dementia, senile dementia and myocardial ischemia, etc.
WO2008121877A3 Cftr inhibitor compounds and uses thereof The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-6 or encompassed by formulas I-VI) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
CN101669972B Preparation method of capsules for treating breast cancer The invention relates to a preparation method of capsules for treating breast cancer, which comprises the following steps: selecting 45-55 centipedes with a body length of 16+/-1cm, 110-135g of scorpion, 130-150g of ground beetle, and 20-35g of talc powder, mixing the centipedes, the scorpion and the ground beetle putting them into a pan, frying to dry by using low-degree fire, then grinding into powdery, mixing uniformly, and preparing into the capsules. The capsules prepared by the preparation method have remarkable treatment effect for breast cancer and high cure rate, can cooperate with western medicine for a long time, eliminate the toxic and side reaction in the processes of radiotherapy and chemotherapy in western medicine, enhance constitution, promote physical rehabilitation and simultaneously have lower cost due to fewer raw material components.
WO2011138666A1 Quinolylpiperazino substituted thiolactone compounds and process for the preparation thereof The present invention provides compounds of general formulae A, useful as potential anti-tubercular agents against Mycobacterium tuberculosis H37Rv, and drug-resistant Mycobacterium tuberculosis and a process for the preparation thereof. Formula (A).
EP0649429B1 Heteroatomic oligonucleoside linkages Oligonucleotide-mimicking macromolecules that have improved nuclease resistance are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in natural oligonucleotides with three or four atom linking groups provide unique oligonucleotide-mimicking macromolecules that are useful in regulating RNA expression and in therapeutics. Methods of synthesis and use also are disclosed.
WO2006051997A1 Cystein dioxygenase inducer An excellent cystein dioxygenase inducer and a food or beverage which is for use in alleviating abnormal cystein metabolism. The cystein dioxygenase inducer comprises a branched amino acid. Also provided is a medicinal composition containing the inducer. The food or beverage, which is for alleviating abnormal cystein metabolism, contains a branched amino acid.
US6936617 Nitrogen compounds such as 6-chloro-3-ethyl-2-(2-thiazol-2-yl -imidazol-1-ylmethyl)-imidazo(1,2-b)pyridazine used for prophylaxis of nervous system disorders This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
CN102659597A Naproxen eugenol ester medicinal compound and preparation method of naproxen eugenol ester medicinal compound The invention discloses a naproxen eugenol ester medicinal compound and belongs to propionic acid, 2-(6-methoxy group) naphthalin and 2-methoxyl group-4-(2- allyl) phenyl ester. According to the compound, naproxen is used as raw materials, the acylation is carried out, the naproxen with eugenol are subjected to esterification reaction in dissolvent, and the compound is prepared through recrystallization and purification. Through being used as efficient medicinal ingredients, the compound can be prepared into solid preparations, liquid preparations, injections, ophthalmic preparations, ointments, suppositories, film agents, aerosol or external preparations for clinical diseases of anti-inflammatory, antipyretic and analgesics and the like, particularly for diseases caused by infection.
CN101129328A Compound aminophenazone barbital Injection and method of producing the same The invention discloses a compound aminolinbarbitone injection and manufacturing method, which comprises the following parts: 5. 0-5. 3% aminobilin, 2. 0-2. 2% analgesine, 0. 9-1. 0% barbitone, 0. 0014 -0. 0018% disodium calcium ethylene diamine and injecting water. The manufacturing method of compound aminolinbarbitone injection comprises the following steps: injecting 5. 0-5. 3% aminobilin, 2. 0-2. 2% analgesine and 0. 9-1. 0% barbitone into injecting water; blending; embedding; aerating CO2 into the injecting water until saturating; setting the temperature of the injecting water at 60-70 deg. c; adding complex builder into the injecting water before adding the main drug components; dispensing to stir evenly; aerating CO2 continuously over 30 min; embedding to aerate N2. The invention is added with 0. 05% active char to stir to adsorb over 15 min to add the same batch of drug liquid to refilter and embed, which stabilizes the injection quality.
WO2011082617A1 (e)-1-(3,5-dimethoxyphenyl)-2-(3,5-dihydroxy-4-methoxyphenyl)ethylene and preparation method and use thereof Disclosed are new (E)-1-(3,5-dimethoxyphenyl)-2-(3,5-dihydroxy-4-methoxyphenyl) ethylene with following structure formula (I) and its preparation method and use in the manufacture of a medicament for preventing and/or treating neurodegenerative diseases. It is proved by test that the compound has great protective effect on neurons and can markedly improve the learning and memory disorder in mice induced by scopolamine. Therefore, the compound has likely preventing and/or treating effect on neurodegenerative diseases and has potential use in the fields of pharmaceutics.
CN103249419A Compositions with antibacterial and wound healing activity The present invention relates to compositions based on silver and hyaluronic acidand their use in the management of cutaneous lesions of various origin (acute and chronic wounds, ulcerations, burns, etc.) mainly when characterized by the presence of exudate and hence at high risk of infection.
CN101120926B Freezing-dried preparation containing voriconazole and its preparation method The present invention discloses a voriconazole freezing dry preparation and the preparation method, which comprises the voriconazole, the oiliness component, the emulsifier and the freezing dry preparation. In the present invention, the voriconazole is packageed into the lipid micro sphere by the voriconazole freezing dry preparation. The melting speed is fast and the safety property is reliable.
CN101407505A Antivirus andrographolide derivative and preparation thereof The invention discloses an antivirus andrographolidume derivative and the preparation thereof. The derivative is a 14-deshydroxy-11, 12-didehydrogenation andrographolidume-3, 19-disuccinic acid half-ester rimantadine salt which consists of 14-deshydroxy-11, 12-didehydrogenation andrographolidume-3, 19-disuccinic acid half-ester and rimantadine. The combination ratio of the 14-deshydroxy-11, 12-didehydrogenation andrographolidume-3, 19-disuccinic acid half-ester and the rimantadine is 1:2 or 1:1. The dosage form can be any one of the existing medical dosage forms which are injection solution, transfusion, powder injection, dropping pills, tablets, dispersible tablets, sustained-release tablets, fast disintegrating oral tablets, capsule, soft capsule, granules, emulsion and targeting preparation. The preparation is used for treating upper respiratory tract infection, pneumonia, bronchitis, influenza, and the like, and has obvious effect of improving respiratory state, antibiosis, antipyretic action, antiviral effect and the like. The preparing process is simple and the medicine quality is steady.
CN102846644A Application of natural pentacyclic triterpenoid in preparation of medicines capable of inhibiting activity of blood coagulation factor Xa The invention relates to a natural pentacyclic triterpenoid or pharmaceutically acceptable salts or esters thereof and a pharmaceutical composition including the natural pentacyclic triterpenoid. The pentacyclic triterpenoid can be extracted from a plurality of plants, especially from achyranthes root, hirsute shiny bugleweed herb, white birch, glossy privet fruit, licorice and the like. Based on inhibition of the blood coagulation factor Xa, the pharmaceutical composition including the pentacyclic triterpenoid and pharmaceutically acceptable salts or esters thereof can be effectively used as an anticoagulant for treatment of thromboembolism. The invention also relates to application of the pentacyclic triterpenoid or pharmaceutically acceptable salts or esters thereof in treatment and prevention of diseases which can be treated and prevented through inhibition of the activity of the factor Xa, e.g., thromboembolism, and in preparation of medicines used for treating the diseases. The invention further relates to a composition of the pentacyclic triterpenoid or pharmaceutically acceptable salts or esters thereof and an inert carrier obtained through mixing or bonding.
CN102796093A Thiomorpholine-containing pyrrole derivatives and their preparation method and use The invention belongs to the technical field of antiplatelet drugs and provides thiomorpholine-containing pyrrole derivatives and pharmaceutically acceptable salts thereof. The thiomorpholine-containing pyrrole derivatives have a general structural formula I. In the general structural formula I, m and R are defined in the patent specification. The invention relates to a preparation method of the thiomorpholine-containing pyrrole derivatives, discloses a drug composition containing the thiomorpholine-containing pyrrole derivatives or their pharmaceutically acceptable salts as active ingredients, and also discloses a use of the thiomorpholine-containing pyrrole derivatives and their pharmaceutically acceptable salts in antiplatelet drugs.
WO2009140557A2 Modified release tolterodine formulations Modified or extended release formulations containing tolterodine and associated methods are disclosed and described. Methods for making and administering said modified release formulations are also disclosed.
US20120171307 Magnesium Compositions and Uses Thereof for Neurological Disorders A composition for administration to a subject, such as oral administration to a subject, for example, has been provided. Such a composition may comprise at least one magnesium-counter ion compound. A magnesium-counter ion composition described herein may be useful for any of a variety of applications provided herein, such as maintaining, enhancing, and/or improving health, nutrition, and/or another condition of a subject, and/or cognitive, learning, and/or memory function. A magnesium-counter ion composition provided herein may be useful for administration to a subject presenting magnesium deficiency, mild cognitive impairment, Alzheimer's disease, attention deficit hyperactivity disorder, ALS, Parkinson's disease, diabetes, migraine, anxiety disorder, mood disorder, and/or hypertension. A kit, method, and other associated technology are also provided.
CN102791307A Removal of virulence factors through extracorporeal therapy A method to remove virulence factors from infected blood by passing the blood through a surface cartridge with immobilized carbohydrates, such as heparin, wherein the virulence factors are toxins released from pathogens such as B. anthracis, S. aureus, and P. aeruginosa.
US20090075888 Cardiovascular and Brain Cell Therapy Using Intracellular Ryanodine Receptor Modulation by the Estrogen Receptor Beta The present invention includes compositions and methods for screening for a candidate substance with ryanodine receptor (RyR)-modulatory activity, the method including: determining the ion-conducting ability and ability to change the concentration of the free cytoplasmic intracellular Ca2+ by the RyR modulated by Estrogen receptor-β (ERβ) in cells or cell membranes expressing RyR and ERβ combination with, or in the absence of the estrogen; contacting the cells or cell membranes with a candidate substance capable of modulation the interaction between RyR and ERβ; and measuring the RyR mediated ion-conducting ability of the cells or cell membranes to change the concentration of the free cytoplasmic intracellular Ca2+ by the candidate substance, whereby the modulatory activity of the candidate substance on RyR/ERβ interaction is determined.
CN102151249A Medical composition of vinflunine The invention relates to a freeze-drying medical composition of vinflunine for injection, in particular to a freeze-drying composition which is prepared by adding organic acid in a vinflunine solution and then carrying out freeze-drying. The composition can be stored in shade. The invention also relates to a parenteral medicament prepared from the composition, and the medicament is preferably perfused through the veins and is preferably used for treating tumors.
DE102011013524A1 Gastroprotective agent comprises Exportal, which is 4-O-(beta-galactopyranosyl)-D-glucitomonohydrate) Gastroprotective (antiulcer) agent comprises Exportal(RTM: 4-O-(beta -galactopyranosyl)-D-glucitomonohydrate). - ACTIVITY : Antiulcer; Gastrointestinal-Gen. The antiulcer activity of Exportal(RTM: 4-O-(beta -galactopyranosyl)-D-glucitomonohydrate) (a) was tested in rats using biological assay. The results showed that (a) (300 mg/kg) exhibited reduction in the area of ulcer damage by 1.3+- 0.2 mm 2>compared to control group (3.1+- 0.3 mm 2>). - MECHANISM OF ACTION : None given.
WO2014031403A1 Use of morphine analogs for animal health A method of treating an animal suffering from a painful condition or disease comprising administering to the animal an effective amount of a compound of Formula (I) or pharmaceutically acceptable salt thereof, wherein, the animal is livestock or a companion animal.
CN101822724A Chitosan composition with anti-fatty liver role and application thereof The invention discloses a chitosan composition with anti-fatty liver role and an application thereof, belonging to application technology of chitosan and derivatives thereof. The chitosan composition relates to two chitosan derivatives of O-carboxymethyl chitosan and cetyl-N,N-dimethyl quaternary ammonium salt chitosan, the two derivatives and the chitosan are mixed with salvia miltiorrhiza, tuber fleeceflower root and twotooth achyranthes root powder according to a certain proportion and further pressed into tablets, the tablets are mixed in feeds for rats, the dosage is 0.05-0.25g/day, and the chitosan composition has obvious roles of preventing and treating fatty liver of the rats. The product adopts natural raw materials and has obvious effect of treating the fatty liver of the rats, so that the product is speculated to be used for treating and preventing the symptoms of the fatty liver of human beings.
CN101953829A Application of imperatorin in preparing antineoplastic medicine The invention relates to the technical field of medicine, in particular to a new application of a coumarin compound imperatorin in preparing an antineoplastic medicine. Indicated by in vivo and in vitro pharmacological tests, the coumarin compound imperatorin has definite antineoplastic activity and can be used for preparing the antineoplastic medicine. The imperatorin has convenient preparation, low price, high safety and favorable development and utilization prospects. The invention provides a new use of the imperatorin and also provides a new medicine source for preventing and treating tumor.
US20110213028 Fatty acid mycophenolate derivatives and their uses The invention relates to fatty acid mycophenolate derivatives; compositions comprising an effective amount of a fatty acid mycophenolate derivative; and methods for treating and preventing organ rejection and autoimmune diseases such as systemic lupus erythematosus, psoriasis and multiple sclerosis comprising the administration of an effective amount of a fatty acid mycophenolate derivative.
CN102091033A Ibuprofen nanoemulsion and preparation method thereof The invention relates to ibuprofen nanoemulsion and a preparation method thereof. The ibuprofen nanoemulsion comprises ibuprofen, glycerol triacetate, Tween-80 and water in a mass ratio of (1-5):(5-15):(10-20):(20-100). The preparation method of the solvent comprises: adding ibuprofen into 10 milliliters of glycerol triacetate, and stirring to dissolve ibuprofen; adding Tween-80, and stirring for 2 minutes to dissolve the Tween-80; and adding water till the total volume is 100 milliliters, and stirring till the solution is clear. The ibuprofen nanoemulsion prepared by the method can dissolve in water according to any ratio, so the biological utilization rate of the product is improved greatly; and the ibuprofen nanoemulsion has the characteristic of instant, long and high effectiveness, and can keep an effective blood medicine concentration for a long time in the bodies of livestock.
US20110081333 Apparatus and system for treatment and prevention of bags under eyes A simple, safe and effective invention devices for treating bags under the eyes pressure exerting glasses devices, compress badges, bag pressure adhesive strips, cosmetic pressure adhesive strips; to be put on to prevent, and to reduce the bags under the eyes. They are designed to apply antiwrinkle and other cosmetic and therapeutic agents such as hormones, known therapeutic agents, as well as other pharmaceutical, biochemical, nurticeuticals and biological agents, or compounds to enhance the health and beauty of the eye, strengthen the lower eye lids and to treat many oculopathies which can contribute to the condition. They can be used for the eye makeup cosmetically as adjuvant to eye makeup. The electrical stimulation and electromotive force are incorporated in the invention to strengthen the lower eye lids muscles, to improve the health of the eye lids skin and for the delivery of therapeutic agents to treat various oculopathies.
CN102219752A Novel crystal form D of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide The invention belongs to the pharmacy field, and relates to a novel crystal form D of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide, and a preparation method of the novel crystal form D. The novel crystal form D is characterized in that: (1) an interplanar distance value d determined by an X-ray diffraction powder pattern method is showed in that: characteristic spectral lines of 14.13 A, 9.99 A, 6.63 A, 2.99 A, and 2.47 A are corresponded to characteristic diffraction angles 2[theta] of 6.25 DEG, 8.84 DEG, 13.34 DEG, 30.021 DEG, and 36.337 DEG +-0.2 DEG.
WO2009129983A1 Acid addition salts of prasugrel and pharmaceutical compositions comprising the same The invention relates to acid addition salts of Prasugrel, a process for their preparation and pharmaceutical compositions comprising the same. In particular the application relates to salts of Prasugrel with benzenesulfonic and naphthalinesulfonic acids.
EP2545914A1 2-amino-2-oxoethyl trans-3-[5-(6-methoxy-naphtalen-1-yl)-1,3-dioxan-2-yl]propyl-carbamate for use in the treatment of persistent cancer pain The present invention relates to 2-amino-2-oxoethyl trans-3-[5-(6-methoxy-naphtalen-1-yl)-1,3-dioxan-2-yl]propyl-carbamate (hereinafter referred to as compound A) for use in the treatment of persistent cancer pain, alone or as adjunctive treatment
US20070231352 Mucoadhesive thermoresponsive medicament-carrier composition This invention relates to a medicament-carrier composition for use in delivering medicaments or fixing the action site of biological active compounds, which mainly comprises a mucoadhesive polymer and a thermoresponsive polymer. The medicament-carrier composition according to this invention is quite suitable for use in topically delivering biological active compounds, especially those useful in photodynamic diagnosis or therapy, e.g. 5-aminolevulinic acid (called as “ALA” for short).
WO2006128268A8 Ureidic compounds, pharmaceutical compositions containing the same and their use on the treatment of inflammatory diseases The present invention describes functionalizeds derivatives of ethyl 6-N- alkyl and/or 6-N-aryl ureas [1 ,3]dioxolo[5,4-g]quinolin-7-carboxylate (3a-z, 4a-z) and similar types (5a-z), of general formula (I, II, III and IV), useful in the treatment and/or prevention of inflammatory diseases, such as acute or chronic inflammatory conditions, different types of arthritis, asthma, Crohn's Disease and diabetes mellitus Type I, among others. These derivatives have the ability of modulate the inflammatory process, acting in mitogen activated protein kinase p-38 (MAPK-p38). Moreover, the derivatives of the present invention present expressive anti-inflammatory properties evaluated in in vivo models. The present invention also discloses processes for the production of such derivatives and harmaceutical com ositions containin the same.
CN101559140A Micelle solution for immune regulation The invention discloses a micelle solution for immune regulation, which relates to the field of products for immune enhancement and/or immune regulation. The micelle solution is prepared from lycium barbarum polysaccharides or extracts containing lycium barbarum polysaccharides from lyciuml plants of solanaceae. The lycium barbarum polysaccharides are preferably treated by deconcentration and are especially prepared into the micelle solution within a certain range of particle sizes, so that the absorptivity of mucous membranes for the lycium barbarum polysaccharides in oral administration is improved or the allergization of an organism for the lycium barbarum polysaccharides in injection is reduced, therefore, the micelle solution achieves the functions of immune enhancement and/or immune regulation.
CN1768769A Wart resistor The invention provides a wart-removing medicament, which comprises (by weight ratio) 10% false sumac oil, 1% fastocaine powder, 1% dicynone powder and 88% medicinal ethanol.
CN101596266A New article for treating dermatosis and preparation method The invention discloses a new article for treating dermatosis and a preparation method. The raw materials of the article comprise Jidesheng Sheyao tablets, dexamethasone and chlorpheniramine; vaseline is additionally added as a matrix. The production method is to produce ointments according to the components.
CN101921271A Pyridine [2,3-d] pyrimidone compounds and application thereof to pharmacy The invention relates to 3-substituted pyridine [2,3-d] pyrimidone compounds, belonging to the field of medicaments, wherein R1, R2, R3 and X are defined in the specification. The invention also relates to a preparation method of the compounds and application of the compounds in the preparation of drugs for resisting tumors.
US7285525 Suppression of immune response via inhibition of cathepsin S Methods and products for suppressing a class II MHC-restricted immune response in a mammal, or in mammalian cells, are described. The methods depend upon inhibiting invariant chain proteolysis by cathepsin S from class II MHC/invariant chain complexes, thereby reducing the competency of class II MHC molecules for binding antigenic peptides, reducing presentation of antigenic peptides by class II MHC molecules, and suppressing immune responses. The methods may be employed in the treatment of autoimmune diseases, allergic responses, and organ or tissue graft rejection. Pharmaceutical and therapeutic compositions which are peptide-based inhibitors of cathepsin S are also described.
CN101669915A Oridonin dry emulsion and preparation method thereof The invention discloses oridonin dry emulsion and a preparation method thereof. The dry emulsion has good stability and can be stored for a long time. The oridonin emulsion after rehabilitation by adding water has small grain diameter, and can be used for intravenous injection, intramuscular injection or oral administration. The dry emulsion preparation can be directly taken orally or used for preparing other preparations, such as tablet, capsule, dried suspension and powdery mist agent. The dry emulsion comprises 0.01-20% of oridonin, 5-80% of grease, 0.5-25% of emulsifying agent and 1-50% ofpropping agent. The preparation method of the dry emulsion comprises a spray drying method, a freeze drying method, a reduced pressure distillation method and a dry absorbing method.
US7115252 For restoration and maintenance of gingival and periodontal health; antiplaque/antitar agents; mouthwash A method and composition for the restoration and maintenance of gingival and periodontal health are provided. The composition includes a potassium as an essential ingredient, which acts as an anti-bacterial agent. In some embodiments, the compositions include an osmotic agent other than potassium.
CN102119931A Novel metformin hydrochloride slow-releasing tablet and preparation method thereof The invention provides a novel metformin hydrochloride slow-releasing tablet and a preparation method thereof. The slow-releasing tablet comprises the following components by weight percent: 66.6%-73.5% of metformin hydrochloride, 30.9%-21.5% chitosan, 2.0%-4.0% of copolymerization and 0.5%-1.0% of superfine silica powder. The dry granulating technique is adopted in the preparation method and thepreparation method comprises the following steps: uniformly mixing the metformin hydrochloride, chitosan, copolymerization and superfine silica powder in proportion according to the prescription, granulating by using a dry granulating machine, adding superfine silica powder and uniformly mixing, and then pressing the mixture into tablet, thereby acquiring the novel metformin hydrochloride slow-releasing tablet.
WO2005078081A1 Use of compounds that regulate hdac6 tubulin deacetylase activity in the preparation of pharmaceutical compositions, method of identifying the aforementioned regulating compounds, said pharmaceutical compounds and applications thereof The invention relates to the use of a compound that regulates, inhibits or activates the tubulin deacetylase activity of protein HDAC6 in the preparation of novel medicaments for the prophylaxis and treatment of diseases in mammals, preferably humans, which present with alterations in the immunological system and preferably with altered T-lymphocyte activation. The invention also relates to a method of identifying the aforementioned regulating compounds, as well as the pharmaceutical compositions or medicaments used for the prophylaxis and treatment of diseases which present with alterations in T-lymphocyte activation. Said medicaments can be used in a method for the prophylaxis and treatment of a person suffering from an immunological disease, such as genetic or acquired immunodeficiencies, in vaccination processes, autoimmune or inflammatory diseases.
WO2014153394A1 Cellular delivery of dna intercalating agents Compositions and methods for targeted delivery of active agents to cells are provided. The compositions comprise a wholly or partially double-stranded synthetic DNA carrier, and an active agent intercalated in double- stranded portions of the DNA carrier. The DNA carrier may also be linked to a targeting agent. The compositions are useful for delivering an active agent into a targeted cell type, for example a cytotoxic agent.
EP2239262A2 Fused ring heterocycle kinase modulators The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity.
US20120309731 Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.
US7199152 TNF-α production inhibitor comprising kavalactone as an active ingredient The present invention provides a TNF-α production inhibitor containing a kavalactone as an active ingredient, which inhibitor has high safety, exerts an excellent effect of inhibiting TNF-α production, and is useful as a drug or an animal drug for preventing, ameliorating, or treating diseases such as cachexia attributed to cancer or infectious diseases, chronic rheumatoid arthritis, inflammatory diseases, osteoarthritis, systemic lupus erythematosus (SLE), rejection during bone marrow transplantation, multiple organ failure, AIDS, meningitis, hepatitis, and type-II diabetes. The present invention also provides a preventive, ameliorating, or therapeutic agent for diseases caused by abnormal production of TNF-α, the agent containing a kavalactone as an active ingredient.
CN101748124B siRNA segment and application thereof used for curing and/or preventing Peste des petits ruminants The invention provides a siRNA segment and application thereof used for curing and/or preventing Peste des petits ruminants. Both the siRNA segment and a carrier comprising the siRNA segment play the protection role on the Vero clones inflected by Peste des petits ruminants virus (PPRV); the siRNA segment and the carrier comprising the siRNA segment are discovered to be capable of reducing the mRNA level of PPRV-L protein by about 20 percent-40 percent through real-time quantitative PCR and immunoblot assay; therefore, the siRNA segment and the carrier comprising the siRNA segment of the invention can be used for preparing drugs used for curing and/or preventing Peste des petits ruminants, and have important values on curing Peste des petits ruminants with genes.
CN101647899B Medicine for treating barrenness of milk cow The invention discloses a medicine for treating barrenness of a milk cow, which is prepared from 30 of Chinese angelica root, 24 of white peony root, 30 of astragalus root, 30 of white atractylodes rhizome, 24 of tuckahoe, 30 of prepared rehmannia root, 30 of scurfy pea, 30 of chinese dodder, 30 of deerhorn gelatin, 24 of cinnamon, 24 of cumin, 24 of chuanxiong rhizome, and 90 of fluorite. The medicine for treating barrenness of milk cow has the advantages of no toxic and side effects, low price and high cure rate, the total effective rate is 96%, and the cure rate is 90%.
US7276512 anti-tumour properties; surprising in vitro and in vivo cytotoxic activity A compound selected from those of formula (I): wherein: X and Y represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, alkyl, trihaloalkyl and NRaRb, wherein Ra and Rb are as defined in the description R1 represents hydrogen or alkyl R2 represents a group selected from hydrogen, alkyl, —OR″a, —NR′aR′b, —O-Ta-OR″a, —NR″a-Ta-NR′aR′b, —NR″a—C(O)-TaH, —O—C(O)-TaH, —O-Ta-NR′aR′b, —NR″a-Ta-OR″a, —NR″a-Ta-CO2R″a and —NR″a—C(O)-Ta-NR′aR′b, wherein R′a, R″a, R′b and Ta are as defined in the description R3 and R4 represent hydrogen or alkyl A represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH—, —C(O)—CH(R8) or —CH(R8)—C(O), wherein R5, R6, R7 and R8 are as defined in the description its isomers, N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.
CN102757424A 2-benzyl-substituted-benzofuran-imidazolium compounds and preparation method thereof The invention discloses a series of 2-benzyl-substituted-benzofuran-imidazolium compounds and a preparation method thereof. The preparation method comprises the following steps: synthesizing raw materials 2-bromoacetophenone and salicylaldehyde into 2-benzoyl-substituted-benzofuran in an acetone solvent; reducing the 2-benzoyl-substituted-benzofuran into 2-benzalcohol-substituted-benzofuran with sodium borohydride in an alcoholic solution, converting into methylsulfonate, carrying out reflux reaction in a solvent, such as imidazole, 2-methylimidazole or the like, to obtain 1-(2-benzyl-substituted-benzofuran)imidazole, and carrying out reaction with halide to obtain the 2-benzyl-substituted-benzofuran-imidazolium compounds. The design and synthesis of antineoplastic drug molecules are performed by using pharmacophore with obvious antitumor activities in the natural product as a precursor; the synthesized compounds have favorable in-vitro activities for resisting tumor cell toxicity; and when the imidazole structure unit is benzimidazole, 3-substituted-aromatic ring-formylmethyl-imidazolium compound, and especially naphthoyl-methyl-imidazolium compound, the 2-benzyl-substituted-benzofuran-imidazolium compounds have favorable in-vitro anticancer physiological activities.
WO2006068991A1 Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, R0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from -(C1-C4) alkylene-, -S-, -CH(OH)-, or -O-; A is methylene, -S-, -O-, or -NH-; and the other substituents are as defined in the claims.
CN103169705A Compound orally disintegrating tablet containing chlorpheniramine and dextromethorphan The invention relates to a compound orally disintegrating tablet containing chlorpheniramine maleate and dextromethorphan hydrobromide and a preparation method thereof. The compound orally disintegrating table comprises covered granules containing chlorpheniramine maleate, dextromethorphan hydrobromide and at least one stabilizer, a filling agent, a disintegrating agent and a lubricating agent. The compound orally disintegrating tablet provided by the invention is good in stability, high in dissolution rate, simple in preparation technology and environmentally friendly.
WO2011088715A1 Use of albiflorin for anti-parkinson's disease Use of albiflorin in preparation of medicaments or health care product for preventing, alleviating and/or treating parkinson's disease. The trials of the present invention prove that albiflorin has distinguished anti-trembling effect and low toxic and side effect.
US20080182818 Th1 CELL DIFFERENTIATION ACCELERATOR The present invention provides an agent for promoting human Th1 cell differentiation and an agent for suppressing human Th2 cell differentiation, comprising lipoarabinomannans and/or lipomannans derived from BCG cell bodies. The agent of the present invention is useful as a prophylactic/therapeutic agent for cancers and the like, and also as a therapeutic agent for allergic diseases such as pollinosis.
US20070287680 Combined Active and Passive Targeting of Biologically Active Agents Disclosed is a conjugate comprising a biologically active agent (drug) linked to a subcellular targeting moiety that targets a drug specifically to the nucleus. Targeting is achieved by attaching a steroid hormone (or an analog) to the drug. The steroid hormone attached to the drug binds its corresponding receptor, the formation of the receptor-ligand complex results in the internalization of the complex into the nucleus, thus resulting in nuclear translocation of the drug. Also disclosed is a conjugate (comprising the complex of the drug and the steroid hormone) bound to a polymer by spacers allowing for concurrent passive targeting to the tumor cell (afforded by attachment to the polymer by the EPR effect) and nuclear targeting of the conjugate (due to the presence of the steroid). Using a suitable degradable spacer allows for the release of free drug in the tumor and enhances nuclear targeting efficacy. The polymer can be further linked to a cellular targeting molecule, where the targeting molecule directs the polymer to specific cells. One may thus be able to effectively target drugs to the nucleus of tumor cells. With little or modifications, several therapeutic agents can be targeted using the invention.
CN103142701A Ear dropping oil agent for mixed infection of pet ear canal and preparation method thereof The invention discloses an ear dropping oil agent for mixed infection of a pet ear canal and a preparation method thereof, and aims to provide an ear dropping oil agent for mixed infection of a pet ear canal, which is simple in preparation method, convenient to use, good in curative effect and high in safety. The technical point provided by the invention is as follows: the ear dropping oil agent for mixed infection of the pet ear canal is composed of the following components in parts by weight: 0.1-1 of ciprofloxacin, 0.1-1 of metronidazole, 0.05-0.5 of phoxim, 0.05-0.5 of lidocaine, 0.5-2 of tea tree oil, 60-80 of glycerol, and 20-40 of distilled water; and the ear dropping oil agent for mixed infection of the pet ear canal belongs to the technical field of animal medicines.
US20110288074 New adenosine receptor ligands and uses thereof The present invention provides new compounds with high affinity for adenosine A2A receptors. It also provides antagonists of adenosine A2A receptors and their use as medicaments for the treatment and/or prophylaxis of diseases and disorders where the partial or total inactivation of adenosine A2A receptors signalling pathways could be beneficial such as Alzheimer's disease, Parkinson's disease, attention deficit and hyperactivity disorders (ADHD), Huntington's disease, neuroprotection, schizophrenia, anxiety and pain. The present invention further relates to pharmaceutical compositions containing such new compounds with high affinity for adenosine A2A receptors and their use for the treatment and/or prophylaxis of diseases and disorders where the partial or total inactivation of adenosine A2A receptors could be beneficial
WO2014052836A3 Methods and compositions for treating infection Provided herein are compositions and methods for treating or preventing infection.
EP2037927A1 Flibanserin for the treatment of urinary incontinence and related diseases The invention relates to the use of Flibanserin for the treatment or prevention of urinary incontinence and related diseases. In a further embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment or prevention of urinary incontinence and related diseases.
WO2014139512A1 Derivatives of indoles and carbazoles, method for the production thereof and use thereof as mrsa-sensitive antibiotics The 1,3-bis(indol-3-yl)-tetrahydrocyclopenta[b]indoles, 1,4-bis(indol-3-yl)tetrahydrocarbazoles, 6,10-bis(indol-3-yl)hexahydrocyclohepta[b]indoles, 6,11-bis(indol-3-yl)hexahydrocycloocta[b]indoles and 11-(indol-3-yl)benzo[b]carbazoles of the general formulae and developed in accordance with the invention have a selective inhibiting effect on the growth of S. aureus and the methicillin-resistant S. aureus (MRSA) in the lower micro-molecular concentration range in a screening of additional Gram-positive and Gram-negative bacteria and fungi. The production of the compounds from dialdehydes and indoles at room temperature in glacial acetic acid constitutes a protective method in which the new structures are available with very good yields in some cases.
EP2561876A1 Formulations of Deoxycholic Acid and Salts Thereof The present application is directed to an aqueous pharmaceutical composition comprising from about 0.4% w/v to less than about 2% w/v of a salt of deoxycholic acid, wherein the composition is maintained at a pH from about 8.1 to about 8.5 such that the composition is stabilized against precipitation. Also disclosed herein, are methods for stabilizing an aqueous pharmaceutical composition comprising from about 0.4% w/v to less than about 2% w/v of a salt of deoxycholic acid against precipitation, said method comprising maintaining pH of the solution from about 8.1 to about 8.5.
US20120015915 Formulations of 14-epi-analogues of vitamin d The present invention provides new formulations of 14-epi-analogues of vitamin D, such as inecalcitol, providing improved absorption profile.
US20130030006 Agent for preventing or treating diseases accompanied by urinary pain [Problem] Provided is an agent for preventing or treating diseases accompanied by urinary pain. [Means for Solution] A pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or a salt thereof was confirmed to have not only an action of increasing effective bladder capacity but also an analgesic action against bladder pain and testis pain, based on FAAH inhibitory action. Accordingly, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or a salt thereof can be used for preventing or treating interstitial cystitis/bladder pain syndrome and/or chronic nonbacterial prostatitis/chronic pelvic pain syndrome.
US20110300182 Nucleic acid drug for treatment of allergic disease This invention provides double-stranded (ds) RNA capable of suppressing the expression of STAT6 related to allergic diseases mediated by Th2-type cytokines via RNA interference and a pharmaceutical composition for prevention or treatment of allergic diseases comprising such dsRNA. Such dsRNA is a double-stranded RNA (dsRNA) molecule targeting mRNA of the STAT6 gene composed of (a) or (b): (a) a sense strand identical to a sequence having 15 to 50 continuous nucleotides in the STAT6 gene sequence represented by SEQ ID NO: 1 or 3 and an antisense strand comprising a nucleotide sequence complementary to the nucleotide sequence of the sense strand; or (b) a sense strand comprising a sequence derived from the sequence comprising 15 to 50 continuous nucleotides of the STAT6 gene sequence represented by SEQ ID NO: 1 or 3 by deletion, substitution, or addition of 1 or several nucleotides and capable of hybridizing to the STAT6 gene and an antisense strand comprising a nucleotide sequence complementary to the nucleotide sequence of the sense strand.
WO2006053785A1 Radiolabelled quinoline-based ligands for the 5-ht6 receptor functionality The present invention relates to radiolabelled compounds of formula (I), which are useful for the labelling and diagnostic imaging of 5-HT6 receptor functionality, and the treatment of CNS related disorders.
CN101914106A Cefamandole nafate hydrate and preparation method thereof The invention relates to a cefamandole nafate hydrate. The molecular formula of the cefamandole nafate hydrate is C19H17N6NaO6S25H2O. The preparation method of the cefamandole nafate hydrate comprises the following steps of: dissolving cefamandole nafate crude drug in water and placing the dissolved cefamandole nafate crude drug in a crystallizer; adding 5-15 parts of elution agents, cooling the mixture to 2-8 DEG C, separating out solids and then filtering; and rinsing the solids in the elution agents, drying for 3-5 hours at the drying temperature of 10-50 DEG C under a ventilated or vacuumcondition to obtain the cefamandole nafate hydrate. The invention also provides a cefamandole nafate for injection, which is prepared by using the cefamandole nafate hydrate as the crude drug. The cefamandole nafate hydrate obtained in the method has the advantages of smooth surface, good stability and high dissolving sped in water. After the cefamandole nafate hydrate is dissolved in the water, the action mechanism and the clinical effect of the cefamandole nafate hydrate are the same as those of cefamandole nafate prepared in the traditional process.
WO2012112548A3 Firmocidin, an antimicrobial molecule produced by staphylococcus epidermidis The disclosure provides for novel antimicrobial agents, methods of making, and methods of use thereof.
US20110027356 Combination of Oral Medicaments Bonded by a Wrapping Oral pharmaceutical dosage form containing at least two medicaments, in which form the medicaments on the one hand are brought together in a leakproof and in-vivo water soluble wrapping and on the other hand are separated so that the active principle of the combined medicaments cannot come into contact with one another, at least one of the medicaments being selected from the following therapeutic classes: non-steroidal anti-inflammatory drug (NSAID), proton pump inhibitor (PPI), beta-blocker, statin, conversion enzyme inhibitor (CEI), biguanide, myorelaxant, calcium inhibitor, corticoid, antidepressant, benzodiazepine, non-atropine-like intestinal transit retarder, intestinal antibacterial, and the following therapeutic molecules: spironolactone, propranolol, clarithromycin, amoxycillin, low-dose acetylsalicylic acid, potassium, clopidogrel.
EP1583536A2 Method of treatment of prostate cancer and composition for treatment thereof A method and composition for the treatment of prostate cancer comprises an effective amount of a nonsteroidal antiandrogen and an effective amount of a selective estrogen receptor modulator. The composition has fewer side effects such as breast tenderness and gynecomastia and also is more effective as an adjuvant therapy to prevent the reoccurrence of prostate cancer.
US20100318040 Catheter Locking Solution Having Antimicrobial and Anticoagulation Properties The present invention includes a catheter locking solution having both antimicrobial and anticoagulant properties including a local anesthetic and a viscosifying agent. The local anesthetic of the present invention may be an amino amide; an amino ester; an aminoacylanilide; an aminoalkyl benzoate; an amino carbonate; an N-phenylamidine compound; an N-aminoalkyl amid; an aminoketone, or combinations and mixtures thereof. In a particular embodiment of the present invention, the local anesthetic is tetracaine or dibucaine.
CN103145863A Method of extracting cynomorium songaricum polysaccharide through enzyme treatment and preparation of cynomorium songaricum polysaccharide antineoplastic agents The invention discloses a preparation method of cynomorium songaricum polysaccharide and a preparation method of cynomorium songaricum polysaccharide antineoplastic agents. The cynomorium songaricum polysaccharide mainly exits in cells or cell walls. According to the preparation method, enzyme agents are added in the extracting process, the cell walls can be degraded under a mild condition, cells without cell walls are broken through high-speed stirring, the release of polysaccharide is promoted, and the effect of improving the extracting rate is achieved. The preparation method improves the extracting rate of the cynomorium songaricum polysaccharide by 10-65% compared with a traditional water extract and alcohol precipitate method, and improves the content of the cynomorium songaricum polysaccharide by 5-40%. The preparation method is simple in process, low in extracting cost, and suitable for industrialized production. The prepared cynomorium songaricum polysaccharid extracted through the method is high in purity, and the ynomorium songaricum polysaccharide agents can be directly prepared and have various effects such as immunity enhancement, fatigue prevention and tumor prevention, and are suitable for tumor patients.
US8088410 25-hydroxy Vitamin D3 compositions An oil composition containing 25-hydroxy Vitamin D3 and an oil is provided. In addition an emulsion, a microencapsulated oil composition, and a feed premix composition each containing 25-hydroxy Vitamin D3 are provided. Methods of making an oil composition, a microencapsulated oil composition, and a feed premix containing 25-hydroxy Vitamin D3 are also provided.
CN1871242A 3-(4-aminophenyl) thienopyrimid-4-one derivatives as MCH R1 antagonists for the treatment of obesity, diabetes, depression and anxiety This invention relates to novel arylamines which are antagonists of the melanin-concentrating hormone receptor 1 (MCH R1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in medicines for the treatment of obesity, diabetes, depression, and/or anxiety. Compounds of the invention have the formula.
US20120040984 Thiadiazole and oxadiazole derivatives, preparation thereof and therapeutic use thereof The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.
EP1743676A1 Heterocyclic boronic acid derivatives, dipeptidyl peptidase IV inhibitors Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH3)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CRiRii, R1, R2, R3, R4 and R5 are as described herein.
CN201200626Y Tablet capsule containing diphosphonates tablet and vitamin D tablet The utility model provides a tablet capsule which makes active components in the tablet capsule to be nonreactive with the tablet capsule. The tablet capsule is composed of a capsule and tablets in the capsule; the capsule comprises an upper capsule body and a lower capsule body, the capsule contains at least one bisphosphonate tablet and a vitamin D compound tablet. The active components of the bisphosphonate tablet and the vitamin D compound tablet are not made of raw materials or auxiliary materials easy to be subjected to physical or chemical reaction with the bisphosphonate tablet and the vitamin D compound tablet. Preferably, the capsule also contains a blank tablet with no active component. Compared with the prior art, the utility model has the advantages that active components cannot be subjected to chemical reaction and by-product generation so that the tablet capsule has high stability; in addition, the utility model is extremely suitable for industrialized production and has good patient compliance.
WO2010019698A3 Inhibition of calicivirus (norovirus) The invention provides a method of treatment or prophylaxis of Calicivirus infection, comprising administering a pharmaceutical composition comprising a compound selected from the group of compounds consisting of interferon-alpha (IFN-α), interferon-gamma (IFN-γ), honokiol, magnolol, ribavirin, z-guggulsterone, and a combination thereof and a pharmaceutically-acceptable carrier to a patient having a Calicivirus infection, or at risk for becoming infected with a Calicivirus.
EP1509217A1 Monotherapy for the treatment of amyotrophic lateral sclerosis with cyclooxygenase-2 (cox 2) inhibitor(s) A method of treating, preventing, or inhibiting ALS, in a subject in need of such treatment, inhibition or prevention. The method comprises administering to a subject one or more cyclooxygenase-2 selective inhibitor(s), or isomer(s), or pharmaceutically acceptable salt(s), ester(s), or prodrug(s) thereof, wherein the amount of the cyclooxygenase-2 selective inhibitor(s), isomer(s), ester(s), salt(s) or prodrug(s) thereof constitutes an ALS treatment, inhibition or prevention effective amount of the COX 2 inhibitor(s).
US7759361 treating a cancer, autoimmune diseases and cardiovscular disorders comprising administering drugs such as Isobutyric acid 2-isobutyryloxymethyl-3-oxo-1-aza-bicyclo[2.2.2]oct-ylmethyl ester; antiproliferative agents Compounds of Formula (1) process for preparing them, pharmaceutical compositions comprising them. The use of compounds of formula (1) for hyperproliferative diseases, e.g. cancer as well as autoimmune diseases and heart disease.
US7378406 11 beta -(4-acetylphenyl)-17 beta-hydroxy-17-alpha-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a derivative, especially for prophylaxis and treatmenet of breast cancer The present invention relates to methods and uses for preventing or treating hormone-dependent disease, in particular breast cancer, in a mammal by antiprogestins, in particular antiprogestin 11β-(4-acetylphenyl)-17β-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof. The invention further relates to pharmaceutical compositions comprising said antiprogestin.
CN102335288A Giant salamander skin mucus scalding ointment The invention discloses scalding ointment prepared from giant salamander skin mucus. A method for preparing the scalding ointment comprises the following steps of: collecting the giant salamander skin mucus in a giant salamander artificial cultivation pond, performing freeze drying under vacuum, and crushing to form 120-mesh mucus powder; crushing rhubarb and giant knotweed rhizome in the ratio of 1:1 to form 80-mesh powder, adding water in an amount which is 30 times that of the powder, and leaching at the temperature of 85 DEG C for 2 hours; and leaching 15 percent of mucus powder and 30 percent of leach liquor at the temperature of 65 DEG C for 1 hour, adding 20 percent of mixed oil (tea seed oil, tung oil and sesame oil in the ratio of 3:2:1), 5 percent of borneol, 10 percent of honey, 20 percent of vaseline and 0.5 percent of cinnamyl aldehyde, and mixing uniformly to form the ointment. The ointment is applied to scalding surfaces to increase collagen, amino acid, natural hormone, vitamins, saccharides, mineral substances and other active substances of wounds, has the effects of resisting bacteria and oxidation, preserving moisture, diminishing inflammation, relieving pain, promoting cell proliferation, accelerating wound healing and the like, and has the characteristics of quick healing of the scalding surfaces and no scars after being used.
CN103588783A Epigambogic alcohol acid, as well as preparation method and medical application thereof The invention relates to a cage poly-isopentene xanthones compound epigambogic alcohol acid, which has antitumor activity. The invention also relates to a preparation method of the epigambogic alcohol acid, and the method comprises the following steps: heating gambogic acid which serves as a raw material, and performing liquid chromatographic separation to obtain the epigambogic alcohol acid. The invention further relates to an application of the epigambogic alcohol acid in preparation of an antitumor medicine.
US20080312299 Imidazole Derivatives as Fructose-1,6-Bisphosphatase Inhibitors and Pharmaceutical Compositions Containing Them Imidazole derivatives of formula (I) wherein R1, R2a, R2b, A, V and W are as defined in the description, as inhibitors of fructose-1,6-bisphosphatase, their preparation process and their use in the prevention or treatment of diabetes, and other diseases where the inhibition of gluconeogenesis, control of blood glucose levels, reduction in glycogen stores, or reduction in insulin levels is beneficial and diseases related to the insulin resistance syndrome.
EP1881833A1 Compositions for the treatment of psoriasis What is claimed are compositions for the treatment of psoriasis, eczema and inflammatory conditions of the skin comprising as an active ingredient a therapeutic effective amount of thiamine or its cosmetically and/or toxicologically acceptable salts.
US20100330030 Vasculostatic Agents and Methods of Use Thereof Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as retinopathies or macular degeneration or other vitreoretinal diseases, inflammatory diseases, vascular leakage syndrome, edema, transplant rejection, adult/acute respiratory distress syndrome (ARDS), and the like.
WO2013051597A1 Cephem derivative having catechol group A compound represented by formula (I) or a pharmaceutically acceptable salt thereof. (In the formula, A represents a group represented by one of formulae (i)-(iii); B represents a group represented by formula (v) or (vi); and E represents a substituted or unsubstituted heterocyclic group having a cationic nitrogen atom.)
EP2311463A1 Analogs of galanthamine and lycoramine as modulators of nicotinic receptors Analogs of galanthamine and lycoramine are useful in modulating nicotinic receptors in humans and other animals. Modulation of such receptors is useful in treatment and/or prevention of a number of conditions including treatment of attention disorders, assistance in giving up smoking, and in treatment of Parkinson's disease.
CA2631232A1 Novel vinylogous acids derivatives The invention is concerned with novel vinylogous acids derivatives of formula (I) wherein A and R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.
US7476665 Benzodiazepine CGRP receptor antagonists The present invention is directed to compounds of Formula I: I (where variables R 1?, R 2?, R 3?, R 6?, R 7?, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
WO2009026292A1 Dosing methods for treating disease The invention relates to a method for treating disease such as viral infections, tumors, and cancers, comprising administering a TLR7 agonist or TLR7 agonist prodrug according to a cyclical dosing schedule having a dosing period and a resting period. For example, the mmethod encompasses treating disease with: Formula (I) 5-amino-3-(2 '-Q-aceiyl-3'-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one Tosylate according to a dosing schedule of every -other-day or a dosing schedule of three consecutive days of dosing followed by four consecutive days of not dosing.
WO2009000797A1 N-oxides of venlafaxine and o-desmethylvenlafaxine as prodrugs The invention concerns venlafaxine-N-oxide and O-desmethylvenlafaxine-N-oxide as prodrugs of venlafaxine and its major (active) metabolite O-desmethylvenlafaxine respectively, to pharmaceutical compositions containing these N-oxides, to methods for preparing them, and methods for preparing compositions. The invention relates to N-oxide, having formula (1), wherein R1 is H or CH3, and tautomers, stereoisomers, hydrates and solvates thereof. The invention also relates to the uses of the N-oxides and compositions, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with venlafaxine.
CN102342947A Oral solid preparation containing adefovir and entecavir, and application thereof The present invention relates to a novel oral solid preparation. The preparation comprises: 20-40 mg of adefovir or a pharmaceutically-acceptable salt of the adefovir or a pharmaceutically-acceptable ester of the adefovir; 0.1-2 mg of entecavir or a pharmaceutically-acceptable salt of the entecavir or a pharmaceutically-acceptable ester of the entecavir; and a pharmaceutically-acceptable carrier, wherein a weight ratio of the adefovir or the pharmaceutically-acceptable salt of the adefovir or the pharmaceutically-acceptable ester of the adefovir to the entecavir or the pharmaceutically-acceptable salt of the entecavir or the pharmaceutically-acceptable ester of the entecavir is 2-80:1. The formulations of the oral solid preparation comprise tablets, dispersible tablets, capsules, double-layer tablets, oral disintegrating tablets, chewable tablets, drop pills, granules or dry suspension. With adopting the oral solid preparation to treat hepatitis B or hepatitis C, a congenerous or synergistic therapeutic effect is provided, the drug resistance of the virus is reduced, the adverse reaction of the drug is reduced, and the medication compliance of the patient is improved.
CN101190226A Vitamin B2 chewable tablets for dog or cat The invention discloses a vitamin B2 chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the existing tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 5 to 20 percent of vitamin B2.
CN103191135A Acetylsalicylic acid-phenacetin-caffeine sheet composition and preparation technology thereof The invention discloses an acetylsalicylic acid-phenacetin-caffeine sheet composition and a preparation technology thereof. The preparation technology comprises the following steps of 1, screening acetylsalicylic acid, phenacetin, caffeine, citric acid, microcrystalline cellulose, starch, sodium dodecyl sulfate, hydroxypropyl methylcellulose and polyvinylpyrrolidone K30 by a sieve of 80 meshes for next use, 2, by a fluidized drying granulator, preparing acetylsalicylic acid single-phase microsphere particles from the acetylsalicylic acid, a part of the starch and a part of the sodium dodecyl sulfate screened by the sieve of 80 meshes, 3, by the fluidized drying granulator, preparing phenacetin-caffeine mixed microsphere particles from the phenacetin, the caffeine, a part of the starch and a part of the sodium dodecyl sulfate screened by the sieve of 80 meshes, 4, uniformly mixing the acetylsalicylic acid single-phase microsphere particles, the phenacetin-caffeine mixed microsphere particles and the microcrystalline cellulose, and carrying out tabletting. The preparation technology improves stability of the drugs in the acetylsalicylic acid-phenacetin-caffeine sheet composition, reduces free salicylic acid content of the acetylsalicylic acid-phenacetin-caffeine sheet composition, and guarantees product quality stability.
EP2562172A1 Sphaelactone derivatives, their pharmaceutical compositions, preparation methods and uses The present invention provides micheliolide derivatives or salts thereof of formula (I)
US6964983 Compounds that modulate PPAR activity and methods for their preparation This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disipidemia, hypercholesteremia, obesity, eating disorders, hyperglycemia, atherosclerosis, hypertriglyceridemia, hyperinsulinemia and diabetes in a mammal as well as methods of supressing appetite and modulating leptin levels in a mammal. The present invention also discloses methods for making the disclosed compounds.
WO2011133827A2 Method of treating prostate cancer A therapeutic method for treating prostate cancer is disclosed comprising administering to a patient in need of treatment a ruthenium complex salt.
WO2014043647A1 Therapeutic compositions and associated methods Methods and materials for treating various diseases and medical conditions with meso-biliverdin compositions. In addition methods and materials for producing meso-biliverdin are provided where the methods include reacting phycocyanobilin with an amphoteric compound in a solvent to yield meso-biliverdin are provided.
WO2005034965A1 Use of hyaluronic acid for treating sprain and strain The present invention relates to the use of hyaluronic acid in the preparation of a medicament useful for the treatment of sprain or strain in an animal or human by administration of the medicament. The present invention relates also a method to potentiate the concomitant treatment of sprain or strain with other therapies.
EP2684957A2 Double-stranded siRNA targeting cancer antigen eEF2 The present invention provides an siRNA targeting eEF2 and a pharmaceutical composition for the treatment or prevention of cancer comprising said siRNA.
US20090280115 Dihydropteridinones in the Treatment of Respiratory Diseases The present invention relates to the use of dihydropteridinones of formula 1 wherein the groups X, R1, R2, R3, R4, R5, R6 and R7 have the meanings given in the claims and specification, for the preparation of a medicament for the treatment of respiratory diseases.
US20110092524 Agent for Enhancing Corneal Epithelial Barrier Function The invention relates to a pharmacological action of a compound which functions as a PPARγ agonist on the barrier function of the corneal epithelium. A PPARγ agonist such as rivoglitazone, DRF-2593, GW-544 or BMS-298585 exhibits an excellent effect of enhancing the corneal epithelial barrier function in a test for enhancement of corneal epithelial barrier function, and therefore is useful as a preventive agent or a therapeutic agent for ocular infection or ocular unidentified complaint caused by a decrease in the corneal epithelial barrier function. Further, the PPARγ agonist can enhance the corneal epithelial barrier function of diabetic patients, patients with decreased corneal epithelial barrier function due to aging and patients who underwent refractive surgery such as PRK (photorefractive keratectomy) or LASIK (laser in situ keratomileusis) or cataract surgery.
CN103191048A Preparation method of oleanolic acid bioadhesive preparation The invention relates to an oleanolic acid bioadhesive preparation and a preparation method thereof. The preparation is characterized in that the medicine is closely adhered to gastrointestinal mucosa, and penetrates into blood through passive diffusion, such that treatment effects can be performed. The preparation is characterized in that the preparation is mainly composed of oleanolic acid, an adhesive material, a filling agent, and a binding agent, wherein an effective dose of oleanolic acid is 25-120mg. The invention also provides a preparation method and an adhesion force and release degree examining method of the oleanolic acid bioadhesive preparation. Medicine in the oleanolic acid bioadhesive preparation can be closely adhered to gastrointestinal mucosa in gastrointestinal tracts, can be gradually released, and can penetrate into blood. The medicine reaches action sites through systemic blood circulation, and treatment effects are developed. With the preparation, retention time of oleanolic acid in gastrointestinal tracts can be prolonged, medicine dissolution can be improved, such that the medicine can be sufficiently absorbed, and bioavailability of the medicine can be effectively improved.
CN103735564A Medicinal composition for preventing fatty liver and application thereof The invention belongs to the technical field of medicines, and in particular relates to a medicinal composition for preventing fatty liver and application thereof. The medicinal composition is prepared from the following raw materials: friedelan-3 beta-ol, astragalus polysaccharide component A1, resveratrol and ajugol A. The medicinal composition can be used for effectively preventing fatty liver, has the advantages of remarkable treatment effect and stable quality control, and is suitable for long time administration of patients.
CN1810255A Orally taken health article for treating senile dementia The orally taken health article for treating senile dementia includes a mixture comprising ginsenoside Rb1 and protocyanidin; a mixture comprising ginsenoside Rb1, vitamin B12 and folic acid; or a mixture comprising ginsenoside Rb1, protocyanidin, vitamin B12 and folic acid. The orally taken health article has ginsenoside Rb1 as main component, and the synergistic effect of the other components to strength the bioactivity of ginsenoside Rb1 in human body. It can repair damaged cerebral cell and promote the regeneration of cerebral cell to prevent senile dementia. It is safe and has no toxic side effect.
US20060051314 Drug for prevention and/or treatment of constipation and sympton caused by constipation A medicament for preventive and/or therapeutic treatment of constipation and/or a symptom resulting from constipation which comprises magnesium polycarbophil as an active ingredient. The medicament of the present invention can exhibit high efficacy by promoting a normal defecation without causing a side effect such as a watery stool, an overloose stool, or hypercalcemia.
CN1876069A Plague preventive oil and method for preparing same The invention discloses an antiepidemic oil for preventing various epidemic diseases and its preparing process, which is prepared from sesame oil, orpiment, atractylodes rhizome, black soya bean, grassleaved sweetflag rhizome and Chinese mugwort leaf through the steps of water immersing, de-watering, disintegrating into fines, and mixing homogeneously.
US7612035 Inhibition of mitogen-activated protein kinase (MAPK) pathway: a selective therapeutic strategy against melanoma Inhibitors of the MAPK pathway, including MEK-directed proteases and small molecule inhibitors, are cytotoxic to human melanoma cells in vitro and in vivo via apoptotic mechanisms. These compounds are used to kill melanoma cells and to treat subjects with melanoma, either alone or in combination with other therapeutic modalities.
US20060151574 Formulations useful against hepatitis C virus infections The present invention relates generally to chemical compounds and substances which are effective against Hepatitis C virus (HCV) infections. Moreover, the present invention relates to compositions comprising said compounds and/or substances, to methods for preventing HCV infections as well use of the compounds and/or substances for the preparation of compositions useful for the prophylaxis and/or treatment of HCV infections. Useful compounds and substances according to the invention are selenium, selenium salts, Vitamin D3 and retinoids, like all trans retinoic acid and salts thereof, C1-C alkyl amides of all trans retinoic acid and salts thereof, C1-C10 alkyl esters of all trans retinoic acid and salts thereof, 9-cis retinoic acid and salts thereof, C1-C10 alkyl amides of 9-cis retinoic acid and salts thereof, C1-C10 alkyl esters of 9-cis retinoic acid and salts thereof, (E)-4-[2(5,6,7,8-tetrahydro-5,5,8,8-tetra methyl-2-naphthalenyl-1-propenyl)benzoic acid (TTNPB), (4-[5,6,7,8-tetrahydro5,5,8,8-tetramethyl-2-naphthalenyl)carboxamido]benzoic acid (AM-580), N-(4-hydroxyphenyl)retinamide (4-HPR), and 6-[3-(1-adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid (AHPN).
CN103381273A Doxorubicin prodrug, its preparation method and injectable composition The invention discloses a doxorubicin prodrug, its preparation method and an injectable composition. The doxorubicin prodrug is formed by hydrazone key-type connection between MPEG and DOX. The preparation method of the doxorubicin prodrug is simple; requirements on reaction conditions are low; yield is high; and production costs are easier to control. The prodrug has low immunity and can effectively raise water solubility of doxorubicin. In addition, it will take a long time to remove the doxorubicin prodrug in vivo such that action time of the drug can be effectively prolonged. The doxorubicin prodrug has pH sensitivity and can release doxorubicin in situ in an acidic pH environment and simultaneously form PEG. The doxorubicin prodrug composition can be dissolved in an approximately-neutral aqueous solution to form an aqueous solution with stable performance. When pH changes to acid, supermolecule hydrogel can be formed within minutes. Long-acting in situ release of doxorubicin can be achieved. Doxorubicin diffusion can be effectively avoided. Functions of normal cells are influenced. Toxic and side effect of the drug is reduced.
WO2010108843A1 Use of nitrooxyderivative of paracetamol for the treatment of muscular dystrophies The present invention relates to the use of nitric oxide releasing derivatives of paracetamol for retarding or reversing muscular dystrophies such as Duchenne and Becker dystrophies.
US7485327 For use in pharmaceuticals, dietetics and/or cosmetics; anticancer agents; for treatment of vision defects and periodontal disease The present invention relates to a composition comprising Melissa leaf extract that inhibits angiogenesis and matrix metalloproteinase activity. The Melissa leaf extract of the present invention inhibits angiogenesis and activity of matrix metalloproteinase, so that it can be applied to treat or prevent diseases related to angiogenesis and matrix metalloproteinase. The composition of the present invention comprising Melissa leaf extract may also comprise more than one component of the other anti-angiogenic, anti-cancer, anti-inflammatory and anti-aging components. This particular composition comprising Melissa leaf extract can be used for pharmaceutical, dietetic and/or cosmetic purposes.
WO2005100581A1 Novel isochroman compound and use thereof in anticancer agent, etc. Novel isochroman compound pseudodeflectusin that is isolated from marine microbes parasitizing seaweeds and purified, having a chemical structure represented by the following formula (1) and that exhibits high growth inhibiting activity selectively to human carcinoma cell strains, thus being useful as a novel anticancer substance in a pharmaceutical product, functional food, etc.
WO2013183578A1 IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVE AS KINASE INHIBITOR The present invention provides a compound useful in treating tumors by ROS1 kinase enzyme activity inhibitory action and NTRK kinase enzyme inhibitory action, or a pharmacologically acceptable salt thereof. A compound having an imidazo[1,2-b]pyridazine structure represented by general formula (I), a pharmacologically acceptable salt thereof, or pharmaceutical compositions comprising such compounds. (In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined in the present description.)
CN100998598A Application of glycosamine for preparing medicine to relieve chronic pain An application of aminoglucose in preparing the medicines for remitting chronic pain, especially the nervous chronic pain, is disclosed.
US8629134 Enantioselective synthesis of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one and zilpaterol This invention relates to a process for the hydrogenation of a ketooxime to selectively form an aminoalcohol stereoisomer, and, in particular, to a process for the hydrogenation of 4,5-dihydro-imidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or a salt thereof to selectively form a stereoisomer of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one or a salt thereof. This invention also relates to the use of the 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one hydrogenation product or a salt thereof to selectively make a stereoisomer of zilpaterol or a salt thereof, as well as the use of such a zilpaterol stereoisomer or salt in methods of treatment and medicaments for animals.
CN1985832A Lung-targeting cefoperazone microsphere for animal and birds and its preparing method The present invention belongs to the field of veterinary medicine technology, and is especially lung targeting cefoperazone microsphere for animal and its preparation process. The cefoperazone microsphere is prepared with cefoperazone as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving cefoperazone in gelatin solution and adding Span-80 and liquid paraffin through stirring to obtain emulsion; cooling in icy bath to below 5 deg.c and adding glutaraldehyde through stirring for cross-linking and curing; dewatering with isopropyl alcohol and suction filtering; washing with isopropyl alcohol and ethyl ether to eliminate glutaraldehyd, washing with petroleum ether to eliminate liquid paraffin in the surface of microsphere and vacuum drying at room temperature to obtain cefoperazone microsphere. The medicine has raised tissue selectivity, delayed release, raised curative effect and lowered toxic side effect.
CN102442971A Novel febuxostat crystal form and its preparation method The invention discloses an M-type crystal of a compound as shown in the molecular formula I. The X-ray powder diffraction pattern of the crystalline material has characteristic peaks at diffraction angles (2theta) of 4.89 Deg, 6.68 Deg, 7.27 Deg, 11.69 Deg, 12.89 Deg, 13.36 Deg, 16.56 Deg, 23.12 Deg, 23.89 Deg, 25.96 Deg and 26.77+/-0.2 Deg.
CA2365826C Over-coated chewing gum formulations Methods and products for delivering a medicament or agent to an individual are provided. The product includes a coating having a medicament or agent. The medicament or agent is present within the coating that surrounds a gum center (the water soluble portion and a water insoluble base portion). By chewing the gum, the medicament or agent is released from the product. Continuing to chew the chewing gum creates a pressure within the buccal cavity forcing the agent or medicament directly into the systemic system of the individual through the oral mucosa contained in the buccal cavity. This greatly enhances the absorption of the drug into the systemic system as well as the bioavailability of the drug within the system.
US20080058416 Cns Modulators A method is provided for treating a subject in need of therapy for depression, anxiety, impaired cognition and/or pain comprising administering to said subject an amount of a ketogenic material sufficient to produce a ketosis in the subject sufficient to provide anti-depressant effect, cognition enhancing and/or analgesic effect. Preferred materials produce a ketosis is such that the total concentration of acetoacetate and (R)-3-hydroxybutyrate in the blood of the subject is raised to between 0.1 and 30 mM.
WO2007041077A3 Heterocyclic amide derivatives as rxr agonists for the treatment of dyslipidemia, hypercholesterolemia and diabetes The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating RXR mediated disorders. More particularly, the compounds of the present invention are RXR agonists useful for treating RXR mediated disorders.
CN103505421A Duloxetine hydrochloride enteric micropill preparation The invention relates to a duloxetine hydrochloride enteric micropill preparation which is composed of a drug-carrying pill core, an isolating coating layer and an enteric coating layer. When the enteric materials in the prescription adopt common methacrylic acid copolymers, sugar alcohol can be added into the isolating layer to achieve the goal that the active component in-vitro dissolution curve is consistent with a positive control drug (Cymbalta of Eli Lilly and Company). The product has the advantages of high acid resistance, high dissolution speed, high rate and the like; the methacrylic acid copolymers used as the enteric material are easy to purchase and low in cost; and the adopted conventional preparation method is simple in technique and suitable for industrial production, thereby providing a drug with reasonable price and reliable curative effect for patients with melancholia.
US20120277190 Prodrugs of compounds that inhibit trpv1 receptor Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladder overactivity, urinary incontinence, and other disorders caused by or exacerbated by TRPV1.
WO2006126625A1 Pharmaceutical comprising pyrazolone derivative Disclosed is a pharmaceutical which is intended to be administered in such a form that can reduce a renal disorder exacerbated upon the administration of a pyrazolone derivative and an antibiotic in combination. A cerebral protective agent for use in a patient who receives the administration with an antibiotic, comprising a pyrazolone derivative (e.g., 3-methyl-1-phenyl-2-pyrazolin-5-one) or a physiologically acceptable salt thereof or a hydrate or solvate of the derivative or salt as an active ingredient, the pyrazolone derivative or physiologically acceptable salt thereof or the hydrate or solvate of the derivative or salt being administered subsequent to the administration of the antibiotic.
DE102004037911A1 New mixed cage dimers of 4-phenyl-1,4-dihydropyridine derivatives, useful as HIV-1 protease inhibiting anti-HIV agents which also modulate HIV resistance by inhibiting P-glycoprotein Asymmetric mixed cage dimers (I) of 3,5-bis-(hydroxymethyl)-4-phenyl- 1,4-dihydropyridines are new. Dihydropyridine dimers of formula (I) and their salts are new. R1>H or alkyl; R2alkoxycarbonyl, aryloxycarbonyl, alkylcarbonyl or arylcarbonyl; X : alkoxy, OH, alkoxymethyl, CH2OH, H or NH2. An independent claim is included for the preparation of (I). [Image] - ACTIVITY : Anti-HIV. - MECHANISM OF ACTION : HIV-1 protease inhibitor. The mixed cage dimer (Ia) of 1-benzyl-3,5-bis-(hydroxymethyl)-4-pheny l-1,4-dihydropyridine and 3,5-bis-(hydroxymethyl)-4-(4-methoxyphenyl) -1-(tert. butoxycarbonyl)-1,4-dihydropyridine had inhibition constant 600 nM for inhibition of HIV-1 protease and showed 30 times stronger P-glycoprotein inhibiting activity than verapamil at a concentration of 10 mu M in tests in cells expressing P-glycoprotein.
US20090325916 5-aryl indan-1-one and analogs useful as progesterone receptor modulators Compounds of formula I or II and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I, formula II, or formula III.
WO2008146835A1 Composition for promoting equol production in the blood of subject unable to produce equol It is intended to provide a composition effective for the production of equol in the blood which is to be used for a subject being unable to produce equol by metabolizing daidzein in vivo. Namely, a composition or the like for promoting equol production in the blood of a subject being unable to produce equol, which is characterized by comprising a daidzein type isoflavone and non-fat solid milk components, is provided.
WO2007042647A1 Erythrocytes containing 5-fluorouracil (5-fu) and/or oxaliplatinum The invention concerns erythrocytes containing 5-fluorouracil, optionally associated with other active principles such as oxaliplatinum or another platinum derivative for anticancer therapy. The erythrocytes may have been subjected to a chemically or thermally denaturing treatment to promote their recognition by erythrophagocytic cells. The invention also concerns a drug produced from same, useful for treating primitive or secondary 5-FU-sensitive cancers, in particular secondary cancers present in the liver, the spleen, the lungs, the lymph nodes.
US7291454 Comprises antisense olignucleotides, ribozymes, DNA and guide sequences; animal models; genetic engineering; for use in drug screening Disclosed are transgenic animals and transfected cell lines expressing a protein associated with Alzheimer's Disease, neuroectodermal tumors, malignant astrocytomas, and glioblastomas. Also disclosed is the use of such transgenic animals and transfected cell lines to screen potential drug candidates for treating or preventing Alzheimer's disease, neuroectodermal tumors, malignant astrocytomas, and glioblastomas. The invention also relates to new antisense oligonucleotides, ribozymes, triplex forming DNA and external guide sequences that can be used to treat or prevent Alzheimer's disease, neuroectodermal tumors, malignant astrocytomas, and glioblastomas.
WO2009152340A3 Use of 2,3-substituted thiophenes for the treatment of lung inflammation Methods of treating inflammatory lung conditions comprising administering 2,3- substituted thiophenes of the formula (I).
CN102153607A Water soluble camptothecin derivative and medicinal composition containing same The invention relates to a water soluble derivative of camptothecin and a preparation method thereof. The derivative has a structure shown in a formula (I). The derivative of the camptothecin has improved anticancer activity.
US20100016333 Once-a-day (RNA-Polymerase Inhibiting or phenazine) - dihydropteroate synthase inhibiting - dihydrofolate reductase inhibiting antibiotic pharmaceutical product, formulation thereof, and use thereof in treating infection caused by Methicillin-Resistant Staphylococcus aureus Disclosed are once-a-day antibiotic products for treating Methicillin-Resistant Staphylococcus aureus, or “MRSA,” the products comprising: a combination of at least three different antibiotics, wherein one of the at least three different antibiotics is selected from the group consisting of RNA-Polymerase Inhibiting antibiotics or Phenazine antibiotics, wherein one of the at least three different antibiotics is selected from the group consisting of Dihydropteroate Synthase Inhibiting antibiotics, and wherein one of the at least three different antibiotics is selected from the group consisting of Dihydrofolate Reductase Inhibiting antibiotics (alternatively any or all of the aforementioned RNA-Polymerase Inhibiting antibiotics, Dihydropteroate Synthase Inhibiting antibiotics, and Dihydrofolate Reductase Inhibiting antibiotics may be in the form of analogues, derivatives, polymorphs, metabolites, pro-drugs, salts, and/or hydrates of any of the foregoing); optionally in further combination with a resistance inhibitor, preferably a LexA protease cleavage inhibitor.
DE102010012234A1 Pharmaceutical combination preparation, useful to treat cancer, preferably to reduce e.g. nephrotoxicity of cisplatin or platinum complex analog, comprises 12-imidazolyl-1-dodecanol and cisplatin or a platinum complex analog Pharmaceutical combination preparation comprises 12-imidazolyl-1-dodecanol or its salt and cisplatin or a platinum complex analog in a weight ratio of 1 part by weight to 5-400 parts by weight. - ACTIVITY : Cytostatic; Nephrotropic; CNS-Gen.; Antidote; Hepatotropic. - MECHANISM OF ACTION : Cytochrome P450 2E1 (CYP2E1) inhibitor. The CYP2E1 inhibiting activity of the preparation was tested in microsomes of rat using para-nitrophenol hydroxylation assay. The results showed that imidazolyl-dodecanol exhibited an IC 5 0value of 727.06 nM.
CN103159664A Silodosin bulk drug as well as preparation method and medicine composition thereof The invention discloses a beta crystal form silodosin bulk drug as well as a preparation method and a medicine composition thereof. A residual solvent of the bulk drug does not contain normal hexane; calculated by an internal standard method according to a peak area, the content of ethyl acetate in the residual solvent does not exceed 0.5%; calculated by the internal standard method according to the peak area, the content of beta crystal form silodosin in the bulk drug is 98.0%-102.0%; and calculated by a principal component external standard method according to the peak area, the content of total impurities in related substances does not exceed 0.5%. The beta crystal form silodosin bulk drug prepared by the method has low residual quantity of solvents and stable quality, especially does not contain normal hexane and is suitable for industrialized large-scale production.
CN101854954B A methods for preparing the clathrate compound of steroid medicines utilizing hydrotalcite as carrier The invention provides a method for entrapping steroid medicines by using hydrotalcite as a carrier, which belongs to the technical field of using an organic-inorganic composite material as a releaser. The steroid medicine undergoes the high polymer entrapping by utilizing the insertion-layer characteristics of the hydrotalcite, and is inserted into layers of the hydrotalcite, and the releasing conditions of the object product in phosphate and citric acid buffer solution with different pH values are observed. The method has the advantages that the layering nano carrier forming the hydrotalcite entraps the steroid medicine and performs the insertion-layer, the prepared product can be better released in the colon, and simultaneously the absorption of prednisone in gastric juices is overcome.
WO2009094426A8 13,13-dimethyl-des-c,d analogs of 1alpha, 25-dihydroxy-19-nor-vitamin d3 compounds and topical composition dosage forms and methods of treating skin conditions thereof 13,13-Dimethyl-flfes-C,D analogs of lα,25-dihydroxy-19-nor-vitamin D3 compounds and topical composition dosage forms thereof, and methods of treating skin conditions thereof. Exemplary active pharmaceutical ingredients include (lR,3R)-5-[(E)-(S)-11'-hydroxy-5',5',7',11'-tetramethyl-dodec-2'-enylidene]-2-metylene-cyclohexane-l,3-diol, (lR,3R)-5-[(Z)-(S)-11 '-hydroxy-5',5',7',11'-tetramethyl-dodec-2'-enylidene]-2-metylene-cyclohexane-l,3-diol, (lR,3R)-5-[(E)-(R)-l 1 '-hydroxy-5',5',7',11 '-tetramethyl-dodec-2'-enylidene]-2-metylene- cyclohexane-l,3-diol, and lR,3R)-5-[(Z)-(R)-11'-hydroxy-5',5',7',11'-tetramethyl-dodec-2'- enylidene] -2-metylene-cyclohexane- 1,3 -diol.
US20120083505 Use of opioid receptor antagonists for acute treatment of paraphilic arousal states The present invention is directed to an opioid receptor antagonist or a pharmaceutically acceptable salt thereof for use in a method of acute treatment of paraphilic sexual arousal states in patients suffering from paraphilia.
WO2005030754A1 Indole or quinoline derivatives as non-pepticid npy y2 receptor inhibitors useful for the treatment of anxiolytic and depressive disorders and obesity The invention provides novel non-peptidic NPY Y2 receptor inhibitors (I) useful in treating or preventing: anxiolytic disorders or depression; neurological disorders; bone loss; obesity. Compounds of the invention are also useful in the treatment or prevention of inovulation and infertility. Wherein the fused pyrrolidine ring optionally contains a single carbon-carbon double bond or a sing le carbon ring member adjacent to the nitrogen is optionally = O substituted; n is 1 or 2; m is 0, 1, or 2; Y1-Y5 and R1-R3 are as defined herein.
WO2002053143A3 Treatment of erectile dysfunction with rho-kinase inhibitors The invention relates to the treatment of sexual dysfunction by inhibiton of vasoconstricton leading to the relaxation of smooth muscles in male or female erectile tissue. In one aspect, the invention comprises methods for treating male and female sexual dysfunction which comprises administering a composition comprising a compound which attenuates RhoA and/or Rho-kinase activity in an organ subject to sexual stimulation in a pharmaceutically acceptable carrier to an individual in need of such treatment. In one embodiment, the compound comprises an inhibitor of the enzyme Rho-kinase. In other embodiments, compounds targeted to other enzymes involved in phosphorylation of myosin light chain are used. Also described are compositions and kits for performing the methods of the invention.
CN102670550A Pramipexole dihydrochloride osmotic pump type controlled release tablets The invention provides novel pramipexole dihydrochloride osmotic pump type controlled release tablets. Ethyl cellulose and povidone are used as semi-permeable membrane forming materials; and preferably, the tablets have asymmetrical tablet form, so that the aging phenomenon of a semi-permeable membrane can be eliminated, and medicinal residue is reduced. The invention also provides a method for improving the anti-aging performance of the pramipexole dihydrochloride osmotic pump type controlled release tablets. Moreover, the invention also provides application of an ethyl cellulose and povidone composition in preparation of the pramipexole dihydrochloride osmotic pump type controlled release tablets with the anti-aging performance.
CN1875963A A medicine for treating hepatitis and preparation process thereof The invention relates to a medicament for treating acute hepatitis, chronic hepatitis and persistent hepatitis, and process for preparation, wherein the medicament is prepared from silibinin-N-methylglucamine and biphenyldicarboxylate as the main constituent, and right mxtrix through a predetermined processing combinations. Compared with the existing dosage forms, the drop pill preparation has the advantages of short technological process, low cost of production and quick-effectiveness.
US20110045056 Hydrogel co-polymer composition and its uses, for example as a wound dressing The present invention provides a hydrogel composition, preferably for the treatment of wounds, comprising a hydrophilic co-polymer carrying multiple pendant anionic groups, wherein the polymer is derived from a first monomer and a second monomer, wherein both monomers have an octanohwater partition coefficient Log P value of less than 0, and, the Log P value of the first monomer is greater (more positive) than the second monomer. Preferably the difference between the Log P value for the two monomers is at least 0.1, preferably at least 0.2. The difference between the Log P value for the two monomers is preferably less than 2. The weight ratio (w/w) of the first monomer/second monomer in the hydrogel composition is preferably equal to or more than about 1. The pendant anionic groups may be sulphonyl groups, e.g. sulphonic acid groups or salts thereof. The anionic group in both first and second monomers may be in salt form and the counterion for both monomers is preferably the same.
CN102125543A Heparin-free anticoagulant infection inhibitor for hemodialysis and preparation method thereof The invention relates to a heparin-free anticoagulant infection inhibitor for hemodialysis and a preparation method thereof. The heparin-free anticoagulant infection inhibitor is a preparation comprising the following components in parts by weight: 1 part of sodium citrate, 0.001-0.8 part of methylene blue and 0.001-10.0 parts of chondroitin sulfate as well as a proper amount of adjuvant and an excipient optionally. The heparin-free anticoagulant infection inhibitor has synergetic advantages compared with heparin and other species of single-component dialysis anticoagulants, has no toxic or adverse effect contraindications of heparin, is suitable for more target users than heparin, and provides biological protection for dialysis infection (bacterial or viral infection) which easily occurs in medical care personnel and patients and reduces hemodialysis infection of operators and patients. The heparin-free anticoagulant infection inhibitor has the advantages of easily-accessible raw materials, low price, large market and stable supply, and has good application prospects and social and economic benefits.
CN102961749A Application of fibrate drugs used as drugs for inhibiting myopia The invention relates to a method for preparing drugs capable of delaying and inhibiting myopia. The fibrate lipid-lowering drugs, such as Clofibrate, Fenofibrate and Bezafibrate, are used as the myopia drugs for treating myopia by inhibiting the formation of the myopia.
US20080009483 3-{[(2,3-dihydro[1,4]dioxino[2,3-c]pyridin-7-ylmethyl)amino]methyl}-N-[3-fluoro-6-(methyloxy)-1,5-naphthyridin-4-yl]-4-hydroxycyclopentanecarboxamide; antibiotic resistance; Staphylococcus aureus, Streptococcus pneumoniae and pyogenes, Enterococcus; Haemophilus influenzae, Moraxella catarrhalis, E-coli Napthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed.
US7438934 Administering extractsTribulus terrestris, Epimedium koreanum, Cinnamon cassia Pharmaceutical compositions containing: extracts of Tribulus terrestris, Epimedium koreanum, Cinnamon cassia in the weight ratio of 1.5-3.5:1-2:0.1-0.4 respectively; and optionally arginine or a physiologically equivalent ester, salt or precursor thereof. The compositions are useful in the treatment of male and female sexual dysfunctions. A method of treatment using the pharmaceutical compositions is also described.
US20120027682 Pyrazine Derivatives for Optical Imaging and Therapy The invention provides compounds, including compositions, preparations and formulations, and methods of using and making such compounds. Compounds of the present invention include pyrazine derivatives having a pyrazine core and a plurality of substituents. In some embodiments, pyrazine derivatives of the invention are pyrazine core compounds having one or more electron donating groups and one or more electron withdrawing groups optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.
EP0831892B1 Multimeric, recombinant urease vaccine Methods and compositions are provided for preventing and/or treating Helicobacter (e.g., H. pylori) infection. The compositions of the invention, which are used in the methods of the invention (which include mucosal administration of the compositions), include compositions containing multimeric complexes of recombinant, enzymatically inactive Helicobacter urease in a pharmaceutically acceptable carrier or diluent; and compositions containing (a) a Helicobacter antigen, and (b) an antibiotic, an antisecretory agent, a bismuth salt, or a combination thereof.
CN103704706A Chinese yam and semen plantaginis dispersible tablet and preparation method thereof The invention discloses a Chinese yam and semen plantaginis dispersible tablet. The Chinese yam and semen plantaginis dispersible tablet comprises following components in parts by weight: 200g-400g of Chinese yams, 100g-200g of euryale ferox, 100g-200g of semen plantaginis, 80g-120g of golden cypress, 40g-60g of microcrystalline celluloses, 0.12g-0.32g of crataegus pinnatifida bunge extract, 0.38g-0.78g of calcium carbonate, 0.011g-0.022g of ferrous fumarate, 1g-2g of vitamin C, 1-2 micrograms of vitamin D, 100g-170g of mannitol, 10g-15g of trichlorosucrose, 10g-50g of superfine silica powder, 3g-5g of carboxymethylcellulose, 55g-80g of sodium carboxymethyl starch and 4g-6g of magnesium stearate. The Chinese yam and semen plantaginis dispersible tablet has the effects of tonifying spleen and consolidating Chong vessel, clearing heat and promoting diuresis, increasing the bone density, improving alimentary anemia and the like. The Chinese yam and semen plantaginis dispersible tablet is suitable for morbid leucorrhea, smelly odor and the like, and is used for assisting the recovery.
CN1846701A Multifunctional contraceptive ointment The present invention belongs to the field of medicines, and is especially multifunctional contraceptive ointment. The iodine complex and Wanfujinan in conventional concentration can kill sperm and deactivate HIV, and are prepared into ointment. The ointment is painted inside vagina and penis before sexual intercourse to kill sperm, reach the aim of contraception and kill HIV.
US20060229306 4-(4-Ethylpiperazin-1-yl)-5-methyl-2-phenylthieno[2,3-d]pyrimidine-6-carbonitrile; asthma, atopic dermatitis, chronic obstructive pulmonary disease, Crohn's disease, type I and type II diabetes, lymphoid leukemia and other forms of cancer, multiple sclerosis and autoimmune diseases New 4-aminothieno[2,3-d]pyrimidine-6-carbonitrile derivatives having the chemical structure of general formula (I), and pharmaceutically acceptable salts thereof are disclosed, as well as processes for their preparation and to pharmaceutical compositions containing them and their use in the treatment, prevention or suppression of pathological conditions, diseases and disorders susceptible of being improved by inhibition of PDE7.
US20090082325 Cefidinir Oral Suspension The present invention discloses a novel powder for oral suspension of cefdinir. Also disclosed are methods of preparing the suspension and methods of treatment using the suspension.
WO2007046747A1 Novel bicyclic sulfonamides for use as glucocorticoid receptor modulators in the treatment of inflammatory diseases Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
CN103599087A Rabeprazole sodium enteric-coated pellet and preparation method thereof A rabeprazole sodium enteric-coated pellet is composed of a pellet core, an insulation layer and an enteric-coated layer from the inside to the outside, wherein by the total weight of the enteric-coated pellet, the content of the pellet core is 50 to 70 wt%, the content of the insulation layer is 10 to 20 wt%, and the content of the enteric-coated layer is 20 to 40 wt%; the pellet core comprises rabeprazole, a filling agent, an adhesive, a disintegrating agent, and an alkalizer, by the total weight of the pellet core, the content of the rabeprazole is 7 to 9 wt%, the content of the filling agent is 60 to 75 wt%, the content of the adhesive is 5 to 10 wt%, the disintegrating agent is 4 to 8 wt%, and the content of the alkalizer is 5 to 12 wt%. The rabeprazole sodium enteric-coated pellet has the advantages of low cost, stable quality, and good safety.
US7429576 treatment for osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, breast cancer, endometrial cancer, ovarian cancer and uterine cancer while minimizing undesirable side effects Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3β, 17β-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
US20120004306 External preparation containing analgesic/anti-inflammatory agent An external preparation containing the following components (A), (B), and (C): (A) a non-steroidal analgesic/anti-inflammatory agent, (B) a polyhydric alcohol, and (C) a polyoxyalkylene alkyl ether and/or a polyoxyalkylene alkenyl ether. The external preparation of the present invention has improved the drug efficacy of a non-steroidal analgesic/anti-inflammatory agent, and can be effective at a low concentration. The external preparation of the present invention also has excellent appearance.
CN102824344A Pharmaceutical composition utilizing berberine to inhibit cancer stem cell growth or cancer cell metastasis, and application thereof The invention discloses a pharmaceutical composition for inhibiting cancer stem cell growth or cancer cell metastasis, and application of the pharmaceutical composition. The pharmaceutical composition comprises a berberine compound, and a pharmaceutically acceptable carrier. The application is utilization of berberine compound in preparation of drug for inhibiting cancer stem cell growth or cancer cell metastasis.
CN101007836A Nucleic acid molecule RTN4BSR52 and its application in preparing anticancer medicine The invention belongs to the field of biological pharmacology, and relates to the use of RTN4BSR52 in preparing antitumor medicament, wherein a nucleotide molecule is provided which can be used for preparing antitumor medicaments, wherein the sequence includes TGTATAACCAATGACTGAC or 5'-UGUAUAACCAAUGACUGAC-3', the nucleotide molecule RTN4BSR52 of the invention can be injected into tumors of the nude mice, compared with nude mice injected with other nucleotide molecule under the identical culture conditions, the tumor growth is inhibited appreciably, which is becoming more appreciable with lapses of time. The invention provides a novel approach for the treatment and alleviation of tumor.
US7341716 Solidifying mass in an ionic fluid- containing bodily cavity using polymer comprising 2-cyanoacrylate monomer The present invention provides an occlusive composition comprising: a) a poly(2-cyanoacrylate) monomer of the following formula (I): wherein n≧2 and R is an organic moiety; and b) a visualization agent. The present invention also provides a method for creating a solid mass in an ionic fluid-containing bodily cavity within a living organism, comprising delivering into the bodily cavity a clinically sufficient amount of an occlusive composition comprising a poly(2-cyanoacrylate) monomer of formula (I) and a visualization agent.
US20110092521 Methods of Treating Diseases Using Inhibitors of Nucleoside Phosphorylases and Nucleosidases The invention relates to treating a disease or condition in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase (MTAP) and/or 5′-methylthioadenosine nucleosidase (MTAN). The invention particularly relates to the co-administration of 5′-methylthioadenosine (MTA), or a prodrug of MTA, with one or more MTAP/MTAN inhibitors. Included among the diseases treatable are prostate cancer and head and neck cancer.
CN103405449A Application of Chukrasone A in medicaments for treating breast carcinoma The invention discloses an application of Chukrasone A in preparing medicaments for treating breast carcinoma, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluation finds that the Chukrasone A also has a significant inhibitory effect on the growth of human breast carcinoma cell strains 4T1, MCF-7, MDA-MB-231 and MCF-7B. Therefore, the Chukrasone A can be used for preparing anti-breast carcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating breast carcinoma provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to breast carcinoma cells.
CN102085206A Medicinal composition The invention discloses a medicinal composition, which is characterized by comprising the following bulk pharmaceutical chemicals in parts by weight: 2-32 parts of salvianolic acid A of red-rooted salvia root and 1-8 parts of ginsenoside Rg1, preferentially, 2-32 parts of the salvianolic acid A of red-rooted salvia root and 2-4 parts of the ginsenoside Rg1, or preferentially, 4-16 parts of the salvianolic acid A of red-rooted salvia root and 1-8 parts of the ginsenoside Rg1, or preferentially, 4-16 parts of the salvianolic acid A of red-rooted salvia root and 2-4 parts of the ginsenoside Rg1. Pharmacological experiments show that the medicinal composition provided by the invention has a synergistic effect and a better pharmacological effect as comparison with compositions of effective fractions of ginseng and red-rooted salvia root.
WO2007005531A3 Alkenyldiarylmethanes, fused analogs and syntheses thereof Non-nucleoside inhibitors of HIV-I reverse transcriptase are described. Such inhibitors may be used as part of a combination therapy to treat HIV infection. Compounds described herein exhibit antiviral potency. In addition, compounds described herein exhibit metabolic stability. Also described herein are processes for preparing Non-nucleoside inhibitors of HIV-I reverse transcriptase.
CN101336995A Plaster for treating lumbar intervertebral disc protrusion The invention relates to a sticking plaster for curing lumbar disc herniation. The sticking plaster is prepared from the following components by a certain weight ratio: heracleum hemsleyanum michaux, tiger's bone, carthamus tinctorius linne, salvia miltiorrhiza, frankincense, myrrh, prepared rehmannia rhizome, angelica sinensis, eucommia bark, pseudo-ginseng, vermilion, margarita, rhizoma ligustici wallichii, mercurous chloride, asarum sieboldi, pangolin scales, hemp fruit and turpentine. The sticking plaster has the curative effects of diminishing inflammation, relieving pain, relaxing muscle and tendons, promoting blood circulation, reducing swelling and removing blood stasis, and has the advantages of rapid effect focusing on relieving both secondary and primary symptoms, strong osmotic force, no recurrence after administration and no toxic or side effect. The clinical treatment proves that the sticking plaster has significant curative effects on lumbar disc herniation, cervical spondylopathy, scapulohumeral periarthritis, injury from falling, rheumatism, arthritis and hyperosteogeny with the cure rate of 98% and the effective rate of 100%.
WO2014068585A1 Novel lyophilized compositions of cyclophosphamide The process for producing lyophilized compositions of cyclophosphamide monohydrate, wherein the process does not need rehydration step. The lyophilization is carried out in presence of solvent or mixture of solvent. The compositions of the present invention have greater stability and uniformity.
EP1707568A2 A pharmaceutical composition for use in the treatment of ovarian cancer in a human afflicted therewith The invention relates to a pharmaceutical composition comprising topotecan, for use in the treatment of ovarian cancer in a human afflicted therewith, wherein the composition is for parenteral administration to such human employing a course of therapy of from 1.0 to 2.5 mg (e.g. about 1.5 to about 2 mg) of topotecan/m2 of body surface area per day for about five consecutive days. The invention also relates to a pharmaceutical composition comprising topotecan, for use in the treatment of ovarian cancer in a human afflicted therewith, wherein the composition is for oral administration to such human employing a course of therapy of from 1.5 to 5.0 mg of topotecan/m2 of body surface area per day for about five consecutive days. The pharmaceutical composition can be an oral or parenteral pharmaceutical composition comprising topotecan and an inert, pharmaceutically acceptable carrier or diluent.
CA2339054C E-isomeric fullerene derivatives An E-isomeric fulleropyrrolidine compound of formula (I): (see formula I) is disclosed. Also disclosed is a method for preparing and polymers prepared from such a compound.
EP2543660A1 Prophylactic or therapeutic agent for diabetes or obesity An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the defmitions of the symbols used in the formula).
CN101056981A Method for down-regulating gene expression in fungi The present invention concerns methods for controlling fungus infestation via dsRNA mediated gene silencing, whereby the intact fungus cell(s) are contacted with a double-stranded RNA from outside the fungal cell(s) and whereby the double-stranded RNA is taken up by the intact fungal cell(s). In one particular embodiment, the methods of the invention are used to alleviate plants from fungus pests. Alternatively, the methods are used for treating and/or preventing fungal infestation on a substrate or a subject in need of such treatment and/or prevention. Suitable fungal target genes and fragments thereof, dsRNA constructs, recombinant constructs and compositions are disclosed.
WO2013158046A1 Rnai-based therapies for cardiomyopathies, muscular dystrophies and laminopathies The present disclosure relates to inhibitor of Sun1 for treatment of laminopathies and to Sun1 as markers indicative of a patient's responsiveness to treatment, enabling improved prediction of a patient's risk, monitoring of laminopathies.
WO2014130550A1 Substituted diaryl derivatives as sphingosine receptor modulators The present invention relates to substituted diaryl derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
WO2010022277A2 Combination of 10-propargyl-10-deazaaminopterin and bortezomib for the treatment of cancers The present invention includes a pharmaceutical composition comprising bortezomib and 10-propargyl-10-deazaaminopterin, in a pharmaceutically acceptable carrier. The present invention also includes a method for treatment of T-cell lymphoma in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination comprising bortezomib and 10-propargyl-10-deazaaminopterin.
WO2014066944A1 Treatment or prevention of cardiovascular events via the administration of a colchicine derivative A method for the treatment or prevention of a cardiovascular event in a subject with atherosclerotic vascular disease comprising the step of: b) administering a therapeutically effective amount of a compound of formula (I), a known colchicine derivative and/or a salt thereof R wherein: R1, R2, R3, R4, R9, R10, R11 and R12 independently represent hydrogen, C1-4 alkyl, C2-4 alkenyl, C3-6 cycloalkyl, halogen, C1-4 haloalkyl, nitro, amino, C2-4 acylamino, C1-4 alkyl or dialkylamino, hydroxyl, C1-4alkoxy, C1-4 alkylthio, a group of the formula - SO2N(Rx)2 or SO2Rx where Rx is C1-4 alkyl,C1-4 acyloxy, or optionally substituted phenyl, optionally substituted phenoxy; R7 and R8 independently represent hydrogen, C1-4 alkyl or C1-4 acyl; and R5', R5 ", R6' and R6" independently represent hydrogen, C1-4 alkyl, C2-4 alkenyl, C3-6 cycloalkyl, halogen, C1-4 haloalkyl, nitro, amino, C2-4 acylamino, hydroxyl, C1-4 alkoxy or C1-4 alkylthio a group of the formula -SO2N(Rx)2 or SO2Rx where Rx is C1-4 alkyl, C1-4 acyloxy, or optionally substituted phenyl.
EP1684747A1 Bisindolyl maleimides useful for treating prostate cancer and akt-mediated diseases The present invention provides a method of treating prostate cancer comprising administering to a patient in need thereof a therapeutically effective amount of a compound of the formula (I) wherein R1 and R2 are each independently hydrogen or C1-C4 alkyl; or a pharmaceutically acceptable salt thereof. In a second embodiment, the invention provides a method of treating androgen-independent prostatic adenocarcinoma comprising administering to a patient in need thereof a therapeutically effective amount of compound of formula (I) or a pharmaceutically acceptable salt thereof. In a third embodiment, the invention provides a method of treating an AKT-mediated disease selected from the group consisting of glioblastoma, colon cancer, pancreatic cancer, ovarian cancer, endometrial cancer, and renal cell cancer, comprising administering to a patient in need thereof a therapeutically effective amount of compound of formula (I) or a pharmaceutically acceptable salt thereof.
US8357701 Galactokinase inhibitors Therapeutic agents for treatment of Galactosemia and disorders thereof, and other enzyme related disorders thereof are identified. The compounds inhibit galactokinase (GALK) and other kinase activity and are identified by a high throughput screening assay.
US7217457 Mixture of hydrophobic polymer core and nanoparticles; immobilization The invention relates to composite particles comprising a hydrophobic polymer core and inorganic nanoparticles. Said hydrophobic polymer forms a polymer matrix inside which the inorganic nanoparticles are stabilized and distributed in a relatively homogenous manner. Said particles are at least partially surrounded by an amphophilic copolymer comprising a hydrophobic part and a hydrophilic part, said hydrophobic part being at least partially immobilized in the polymer matrix. The inventor also relates to the preparation method thereof, the conjugates comprising such particles and a ligand and the use of same in reactants and therapeutic compositions.
EP2786986A2 Novel benzamide derivative and use thereof Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc. Further, since it was demonstrated that the present invention displays anti-pruritic efficacy even in an itching model, to which a mechanism and treatment concept established with respect to pain is applied, the present invention may also be effectively used in radical treatment of atopic dermatitis by applying the inventive product to an anti-pruritic composition in order to suppress an initial itching stage and treat symptoms thereof, thus preventing skin damage or inflammation after the scratching stage.
CN103284959A Posaconazole freeze-dried powder injection and preparation method thereof The invention discloses a posaconazole freeze-dried powder injection and a preparation method thereof. The powder injection comprises an active therapeutic ingredient of posaconazole, a solubilizer of cyclodextrin and a pH conditioning agent. An acid is added in preparation processes to form a salt for solubilization. A mixed solvent comprising an organic solvent and injection water is employed, wherein the concentration of posaconazole in the mixed solvent is 2.5 to 15g/ml, the organic solvent is 3.0 to 10.0% by volume, and the balance is the injection water. In the preparation processes, the posaconazole and the acid are stirred or mixed, the organic solvent is added, the mixture is heated stirred or ultrasonically treated to be uniform, the cyclodextrin solution is added, mixture is stirred to be a clear solution, the pH value of the mixture is adjusted, the injection water is added to a constant volume, pyrogens are removed, and then aseptic filtration, subpackaging and freeze-drying are performed. The posaconazole freeze-dried powder injection of the invention has advantages that: the content of the active therapeutic ingredient is high, the stability is excellent, the powder injection is convenient for transport and storage, and the application of the posaconazole in the field of preparations is expanded.
US20080226696 Administerign dosage of carnitine and lipoc acid The present invention provides methods of improving learning ability of aged companion animals (such as aged dogs) by administering an effective amount of a carnitine and an effective amount of a lipoic acid. Also provided are kits and animal treats for improving learning ability of aged companion animals comprising effective amounts of carnitine and lipoic acid.
CN1875944A A carbowax modified stealthy liposome nanosphere of hydroxycamtothecine and preparation method thereof The invention relate to polyethylene glycol modified hydroxycamptothecin stealth greasy nano balls for intravenous injection and its preparing process, which comprises treatment effective amount of hydroxycamptothecin, polyethylene glycol esters, oil for injection, phosphatides and pharmaceutically acceptable auxiliary material by the weight ratio of 0.01-0.2%, 1-10%, 5-25%, 0-10%, 0-10%, and balancing water. The invention also discloses the preparing prcesss including dissolving liposoluble materials into organic solvents, dissolving water-soluble auxiliary materials and addition agents into water, mixing with organic phase, homogenizing or carrying out supersonic treatment.
WO2007073855A1 Use of adenosine a1 receptor agonists for the protection of renal cells against toxic effects caused by aminoglycosides during treatment of infectious diseases The present invention refers to the use of adenosine Al receptor agonists for the protection of renal cells against toxic effects caused by aminoglycosides during treatment of infectious diseases in human.
US7759371 Anticancer, antitumor agents, using 2-amino-5-phenyl- (1,3,4)thiadiazoline compounds (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(═W)R6 or the like; R3 represents a hydrogen atom, —C(═WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
CN103555526A Blueberry yang-invigorating wine The invention is intended to prepare refined pure natural blueberry yang-invigorating wine, which uses liquor, frozen blueberry and frozen lonicera edulis as raw materials, uses fleece-flower root, kiwi berry root, water caltrop, matrimony vine, semen cuscutae, male silkworm moth, epimeddium, cynomorium songaricum, actinolite, morinda officinalis, cistanche, cortex acanthopanacis, Chinese magnoliavine, gen-seng, glutinous rehmannia, broom cypress fruit, hippocampus and pipe-fish as auxiliary raw materials, and maximumly reserves nutrition components of various raw materials by a special technology and a scientific processing method. The blueberry yang-invigorating wine is rich in various vitamins, amino acid, anthocyanidin, flavonod, arbutin and abundant various mineral matter elements, and for long-term drinking, has efficacies of resisting oxidation, aging and cancer, enhancing eyesight, softening blood vessels, enhancing human body immunization, strengthening tendons, tonifying kidney, invigorating yang, etc.
WO2006111348A1 Use of heparin and heparin derivatives for modulating the neurite growth-controlling nogo receptor The invention relates to the use of heparin and heparin derivatives for modulating the Nogo receptor. The invention especially relates to the use of an active substance, selected from heparins and heparin derivatives, for producing a drug for treating diseases or pathological conditions that are accompanied by a disorder of neurite plasticity.
WO2009096817A2 Agent for reducing the degree of acute alcoholic intoxication (inebriation) and the use thereof The invention relates to a novel agent which reduces the degree of acute alcoholic intoxication (inebriation) and exhibits anti-alcohol withdrawal action, to a biologically active additive, pharmaceutical composition and a medicinal agent which decrease alcohol withdrawal syndrome caused by the overconsumption of ethyl alcohol-containing products.
CA2288650C A method for the treatment of mental illness in mammals and a composition therefor The invention relates to a method for treating a mammal suffering from mental illness induced by propagation of stress, said method comprising the step of removing or diminishing the tone of the endogenous alpha-2C-adrenoceptors in the central nervous system of said mammal. The invention relates further to pharmaceutical compositions useful for said treatment.
US20050036951 Methods of treating lung diseases The present invention discloses compositions and methods for treating lung diseases. In preferred embodiments the methods involve administering to the subject via a pulmonary, oropharyngeal, or nasopharyngeal route a compound or composition that contains a therapeutic agent and a targeting element directed to a ligand. The ligand is preferably an epitope on pIgR receptor.
CN103099813A Preparation method and applications of deoxymononucleotide natrium-containing drug composition and preparation thereof The invention discloses a deoxymononucleotide natrium-containing drug composition and applications thereof, and belongs to the technical field of medicine. The deoxymononucleotide natrium-containing drug composition contains deoxyribose adenine nucleotide natrium, deoxyribose thymine nucleotide natrium, deoxyribose guanine nucleotide natrium, and deoxyribose cytosine nucleotide natrium, wherein a weight ratio of the deoxyribose adenine nucleotide natrium to the deoxyribose thymine nucleotide natrium to the deoxyribose guanine nucleotide natrium to the deoxyribose cytosine nucleotide natrium is (3-10):(2-13):(2-11):(1-10). The deoxymononucleotide natrium-containing drug composition has excellent effects in clinic, particularly in adjunctive treatments of acute hepatitis and chronic hepatitis.
WO2009123029A1 Blood ammonia level regulator Disclosed is a blood ammonia level regulator comprising α-cyclodextrin as an active ingredient. The blood ammonia level regulator can be used as a therapeutic agent for hyperammonemia or hepatic encephalopathy. The blood ammonia level regulator can also be used as a prophylactic agent for hyperammonemia or hepatic encephalopathy. The blood ammonia level regulator may be prepared in the form of a preparation for oral administration or enteral administration.
WO2014098516A1 Composition comprising pegylated betulin derivatives, for preventing or treating diaper dermatitis The present invention relates to a composition comprising pegylated betulin derivatives, for preventing or treating diaper dermatitis, and to a disposable absorbent product containing said composition. The composition according to the present invention may effectively prevent or treat diaper dermatitis while causing no skin irritation or side effects, and may have excellent stability and thus can be easily formulated.
WO2009133701A1 Phenylimidazole derivative and therepeutic and/or prophylactic agent for retinal/choroidal disorder Disclosed is a therapeutic and/or prophylactic agent for retinal/choroidal disorders, which comprises at least one member selected from the group consisting of a compound represented by formula (I) and a salt thereof as an active ingredient. [In formula (I), a represents a number of 1 or 2; R0 represents an amino group or the like; R1 to R4 independently represent a hydrogen atom, a C1-6 alkyl group or the like; R5 represents G1 or the like; G1 represents an amino group or the like; b represents an integer of 1 to 4; R6 represents a C1-6 alkyl group substituted by G1, or the like; d represents an integer of 0 to 3; R7 and R8 independently represent a halogen atom or the like; e represents an integer of 0 to 3; the sum total of b and e is 4 or less (i.e., b+e≤4); f represents an integer of 0 to 3; and the sum total of d and f is 3 or less (i.e., d+f≤3).]
US20060134184 At least partially degradable films containing an active ingredient and method for the production of composition comprising an active compound A film which comprises at least one active compound and is at least partly degraded under the conditions of the site of action is suitable as a new presentation form of active compounds, in particular those having a pharmacological or biocidal action.
CN102743508A Compound propolis composition for treating avian infectious laryngotracheitis and preparation method thereof The invention relates to a compound propolis composition for treating avian infectious laryngotracheitis and a preparation method thereof. The compound propolis composition is prepared by mixing 15 to 35 parts by weight of propolis, 25 to 55 parts by weight of gypsum, 15 to 35 parts by weight of folium isatidis, 10 to 35 parts by weight of isatis root, 15 to 35 parts by weight of honeysuckle, 10 to 35 parts by weight of baical skullcap root, 10 to 35 parts by weight of orange fruit, 15 to 35 parts by weight of liquorice, 15 to 35 parts by weight of tatarian aster root, and 10 to 30 parts by weight of borneol. The compound propolis composition has a reasonable formula, can be prepared by simple processes, has no toxic or side effects, does not produce pollution and drug residues, does not cause drug resistance, is crushed into superfine powder, and has high bioavailability and obvious treatment effects. In clinical, the compound propolis composition has special effects of treatment on avian infectious laryngotracheitis.
WO2013011996A1 Polyphosphoric acid composition containing polyphosphoric acid extracted from yeast cell, salt of polyphosphoric acid or solvate of polyphosphoric acid, and method for producing same [Problem] The purpose of the present invention is to provide: a polyphosphoric acid composition which has a high cell proliferation enhancing ability, high cell permeability and a high ability of prolonging the lifetime of a cell and can act to enhance the growth of hair and to maintain the growth phase of hair; a polyphosphoric acid composition which is highly safe and contains a naturally synthesized polyphosphoric acid; and a method for producing a polyphosphoric acid composition containing a naturally synthesized polyphosphoric acid. [Solution] According to the present invention, a polyphosphoric acid composition containing a polyphosphoric acid extracted from an yeast cell, a salt of the polyphosphoric acid or a solvate of the polyphosphoric acid can be produced. The polyphosphoric acid composition containing a polyphosphoric acid extracted from an yeast cell, a salt of the polyphosphoric acid or a solvate of the polyphosphoric acid has high cell permeability. When the polyphosphoric acid composition is applied to skin, gum or scalp, the polyphosphoric acid composition can act effectively for the proliferation of a cell, the prolongation of the lifetime of a cell, the growth of hair, and the maintenance of the growth phase of hair.
US20050182026 Dioleyl phosphatidylcholine (DOPC); distearyl phosphatidylcholine (DSPC) and dipalmitoyl phosphatidylcholine (DPPC) as surface active phosphotidyls; phosphatidyl glycerol, phosphatidyl ethanolamine, phosphatidyl serine, phosphatidyl inositol, or chlorestyl palmitate as spreading agent The efficiency of ultrafiltration in continuous ambulatory peritoneal dialysis (CAPD) is improved by administering a composition comprising at least one surface active phospholipid (SAPL) in powder form, especially as a mixture of phosphatidyl choline and phosphatidyl glycerol, into the peritoneal cavity before commencing CAPD or between CAPD sessions. The SAPL composition may be introduced during surgery to prepare a patient for CAPD and/or subsequently through the incision for the CAPD catheter, or through the catheter itself, between CAPD sessions when one batch of dialysis fluid has been removed and before a fresh batch is supplied.
EP2123269A1 Nanoparticles functionalized with sulfated amino alcohols for the inhibition of selectin-mediated cell adhesion The present invention relates to functionalized nanoparticles inhibiting selectin-mediated cell adhesion and their use as anti-inflammatory therapeutics. More specifically, said functionalized nanoparticles comprise a core, formed by gold, a shell coating said core, formed by a monolayer of a linker molecule, and an acyclic or carbocyclic sulfated amino alcohol linked to said linker molecule via a peptide bond.
WO2008064615A2 Crystalline and amorphous forms of rimonabant and processes for obtaining them Novel crystalline polymorphic Form III of rimonabant and an amorphous form of rimonabant. Crystalline form III of rimonabant is prepared by dissolving rimonabant in an aprotic polar solvent such as acetonitrile or tetrahydrofuran, pouring the solution into water and stirring the resulting mixture. Amorphous form of rimonabant is prepared by dissolving in and alcohol of formula ROH, wherein R is an alkyl, such as methanol or isopropyl alcohol, and stirring the mixture. Rimonabant of formula (I) is obtained in such a way that an ester of 5-(4-chlorophenyl)-l-(2,4-dichlorophenyl)-4-methyl-lH-pyrazole-3-carboxylic acid of formula (III), wherein R is a Cl-C5 alkyl group, phenyl group or a substituted phenyl group, preferably methyl or ethyl, is reacted, in a solvent, preferably in a solvent from the group of diethyl ether, tetrahydrofuran, dioxan, dichloromethane, acetonitrile, toluene or their mixtures, or in an excess of N-aminopiperidine, with N-aminopiperidine with catalysis by at least one Lewis acid at a temperature from 0° C to the boiling point of the solvent or mixture of solvents used. Pharmaceutical compositions containing the above forms and use of the above forms for the manufacture of a medicament the treatment of obesity, for curing of the habit of smoking or for the treatment of Alzheimer or Parkinson diseases are also described.
US20070010458 Drugs for the arthritis treatment Antiinflammatory and/or antiinflammatory/analgesic compounds having the following general formula: A-(B)b0—(C)c0—N(O)s (I) or salts thereof, wherein: A contains the radical of a non steroidal antiinflammatory or non steroidal antiinflammatory/analgesic drug, B and C are bivalent linking groups, are used in the arthritis therapy.
US7906141 Sustained-release, oral pharmaceutical forms of formulation A sustained-release, oral pharmaceutical formulation of tramadol comprising a compound formed in situ of tramadol or its salt and a pharmaceutically acceptable acidic substance. The compound formed in situ has a desired water solubility. Also provided are methods of treatment using the pharmaceutical formulations. Method for preparing such formulations are also provided. The preparation method comprises repeatedly mixing tramadol or its salt with the acidic substance, and moistening the mixture and formulating the mixture under an energy input, such as heat or pressure. Optionally, drying, repeated granulating, extrudation and pelleting may also be included.
US20120252880 Oligonucleotide Complex Compositions And Methods Of Use As Gene Alteration Tools Compositions and methods of treatments of cells are provided for altering the phenotype of a cell by administering an oligonucleotide complex to the cell, the complex having two strands and chemical modifications.
US20090069366 Deuterium-enriched tacrolimus The present application describes deuterium-enriched tacrolimus, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20120165394 Spinal muscular atrophy (sma) treatment via targeting of smn2 splice site inhibitory sequences The present invention is directed to methods and compositions capable of blocking the inhibitory effect of a newly-identified intronic inhibitory sequence element, named ISS-N1 (for “intronic splicing silencer”), located in the SMN2 gene. The compositions and methods of the instant invention include oligonucleotide reagents (e.g., oligoribonucleotides) that effectively target the SMN2 ISS-N1 site in the SMN2 pre-mRNA, thereby modulating the splicing of SMN2 pre-mRNA to include exon 7 in the processed transcript. The ISS-N1 blocking agents of the invention cause elevated expression of SMN protein, thus compensating for the loss of SMN protein expression commonly observed in subjects with spinal muscular atrophy (SMA).
CN1857529A Neogarcinolic acid injection for treating tumor and its preparing method The present invention discloses tumor treating neogarcinolic acid injection and its preparation process. The neogarcinolic acid injection has neogarcinolic acid injection in 1-100 weight portions as the active component, cosolvent 1-100 weight portions, excipient 1-200 weight portions and water for injection 0-5000 weight portions. The preparation process includes the following steps: dissolving neogarcinolic acid in water for injection, adding cosolvent and dissolving, dissolving excipient, adding active carbon through stirring, filtering to eliminate active carbon, and packing. The neogarcinolic acid injection has excellent dissolubility and high stability, and the preparation process is suitable for industrial production and easy product quality control.
CN1548434B Benzothiophene compounds and their preparation and medicine use The present invention discloses one kind of benzothiophene compounds and their preparation process and medicine use. The present invention also discloses their physiologically acceptable salts, their preparation and the application in preparing medicine for preventing and treating women's post-menopause syndromes.
EP1177157B1 A vital matter and a producing method The present invention relates to a vital matter promoting the growth, and increasing preservative capability of human body, animals and plants. The vital matter maximizes active rhythms of human body, animals and plants by inducing sympathy of energy and native wavelenghts between it and animals or plants. In addition, the present invention relates to a producing method of the vital matter composed of the following steps: 1) preparing a composition containing kaoline (white soil) 30-40 wt%, potassium sulfate 15.0-20.0 wt%, sodium sulfate 13.0-17.0 wt%, feldspar 12.0-16.0 wt%, talc 12.0-16.0% and ferric oxide 0.5-1.5 wt%; and 2) mixing the above-mentioned composition using a compressed molding method; and 3) heating the mixed composition at 1000-1300 DEG C. The vital matter of the present invention can be used in whole fields of industries, and will cause the original changes in the field of industrial matters, and promote the welfare of human beings such as improvement of health and life of human.
US7034034 Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives capable of modulating NPY5 receptor activity, are provided. Such compounds may be used to modulate NPY binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.
CA2313633C Method of increasing the production and improving the quality of semen A method of increasing the volume, the total sperm count and the reproductive performance of semen from human and animal males, is described. The method comprises administration of an effective dosage of a human or veterinary preparation containing at least one type of xanthophylls, such as astaxanthin, to said males. Preferably, the astaxanthin exists in a form esterified with fatty acids, e.g. in the form of algal meal produced by culturing of the alga Haematococcus sp. Further, the use of at least one type of xanthophylls, such as astaxanthin, for the preparation of a human or veterinary preparation for increasing the volume, the total sperm count and the reproductive performance of semen from human and animal males, is disclosed.
EP2035009A1 Prolonged improvement of renal function comprising infrequent administration of an aa1ra A method for treating a patient, comprising providing a therapeutically-effective amount of an AA1RA to the patient; and informing the patient or a medical care worker that administration of the AA1RA can provide an improvement in renal function that persists for a time period following administration of the AA1RA, and wherein the time period is at least 3 days.
US7601718 1,5-Dihydro-pyrazolo[4,3-c]pyridazin-6-one derivatives; glycogen synthase kinase-3 (CSK) inhibitors; nervous system, psychological, and neurodegenerative disorders; diabetes, psychiatry, multiple sclerosis (MS), myocardial infarction, reperfusion/ischemia, alopecia, and stroke The present invention provides a compound of formula I: or a pharmaceutically acceptable salt or mixtures thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK mammalian protein kinase, and more particularly inhibitors of GSK-3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
US20110206667 Polymorphism in the apo(a) gene predict responsiveness to acetylsalicylic acid treatment This invention relates to nucleotide polymorphisms in the human Apo(a) gene and to the use of Apo(a) nucleotide polymorphisms in identifying whether a human subject will respond or not to treatment with acetylsalicylic acid.
EP1892250A2 CYR61 compositions and methods Polynucleotides encoding mammalian ECM signaling molecules affecting the cell adhesion, migration, and proliferation activities characterizing such complex biological processes as angiogenesis, chondrogenesis, and oncogenesis, are provided. The polynucleotide compositions include DNAs and RNAs comprising part, or all, of an ECM signaling molecule coding sequence, or biological equivalents. Polypeptide compositions are also provided. The polypeptide compositions comprise mammalian ECM signaling molecules, peptide fragments, inhibitory peptides capable of interacting with receptors for ECM signaling molecules, and antibody products recognizing Cyr6l. Also provided are methods for producing mammalian ECM signaling molecules. Further provided are methods for using mammalian ECM signaling molecules to screen for, and/or modulate, conditions and disorders associated with angiogenesis, chondrogensis, and oncogenesis; ex vivo methods for using mammalian ECM signaling molecules to prepare blood products are also provided. Additionally, modulators, such as peptide modulators, of an ECM signaling molecule activity are provided. Further provided are methods for screening for modulators of a Cyr61 polypeptide-integrin receptor inteaction, as well as methods of treating conditions and disorders associated with such an interaction.
CN101269061A Methoxy flavonoid compound as medicament for preventing and controlling metabolism complex disease and using method The invention discloses a methoxyl flavonoids compound used as a drug for preventing and treating MS (metabolic syndrome) and the usage. As for high-risk MS groups or patients diagnosed with MS, an effective dose of methoxyl flavonoids or compound preparations containing the substances can be adopted for a prevention and/or treatment.
EP0991654B1 Novel 2-(iminomethyl)amino-phenyl derivatives, preparation, application as medicines and compositions containing same The invention concerns novel 2-(iminomethyl)amino-phenyl derivatives, their preparation, their application as medicines and compositions containing them.
CN101554370A Syringin for injection, preparation method and application thereof The invention relates to a syringin for injection, a preparation method and the application thereof. The invention can provide an injection that is clinically and safely used and has the pharmacological actions of resisting fatigue, tranquilizing and allaying excitement, expanding blood vessel, reducing blood viscosity, stanching, and the like. The injection contains syringin, pharmacology-permissible pH regulating substance, a stabilizing agent and an excipient. 50-2800 mg dry substance in each injection contains 5-2000 mg of syringin, 0.04-0.8 g of excipient and 0.0001-0.1g of stabilizing agent. Of the above substance, the pH regulating substance has an adding amount for regulating the weight fraction pH value to 3.5-7.5. The product of the invention is used for preparing medicaments for resisting fatigue, tranquilizing and allaying excitement, expanding blood vessel, reducing blood viscosity, stanching, resisting dumps.
US20120115809 Use of an acylated octasaccharide as an antithrombotic agent The instant invention relates to the use of the octasaccharide of formula (I), wherein Ac represents an acetyl group: in its acid form or in the form of any of its pharmaceutically acceptable salts, for the treatment and prevention of thromboses.
EP2718296A1 Synthesis and characterization of second generation benzofuranone ring substituted noscapine analogs Compounds of Formula (I) and use thereof as microtubule modulating agents in the treatment of cancer are described herein:
US20090092648 Antimicrobial polymer compositions and the use thereof An antimicrobial composition. The antimicrobial composition includes a complex of an anionic polyester with a monomeric amidoamine a complex of an anionic polyester with a monomeric amidoamine or an organic cation, wherein the monomeric amidoamine comprises: (R1,2)N—R3—NH—CO—R4 wherein: R1═H, Alkyl, Aryl, HO—(CH2CH2—O—)n—, MeO—(CH2CH2—O—)n—, HO—(CH2)n—; R2═H, Alkyl, Aryl, HO—(CH2CH2—O—)n—, MeO—(CH2CH2—O—)n—, HO—(CH2)n—; R3=Alkyl, Aryl, —(CH2CH2—O—)—(CH2—)n; R4=Alkyl, Aryl, —(CH2CH2—O—)—(CH2—)n—CH3, —O—CH3, —O—C2H5, —O—C3H7; and n=1-30; and wherein the organic cation comprises: wherein: R1═H, Alkyl, Aryl, HO—(CH2CH2-O—)n-, MeO—(CH2CH2-O—)n-, HO—(CH2)n-; R2═H, Alkyl, Aryl, HO—(CH2CH2-O—)n-, MeO—(CH2CH2-O—)n, HO—(CH2)n-; R3═H, Alkyl, Aryl, —(CH2CH2—O—)—(CH2—)n; R4,5═H, Alkyl, Aryl, —(CH2CH2—O—)—(CH2-)n-CH3, —O—CH3, —O—C2H5, —O—C3H7; and n=1-30; and the anionic polyester is selected from the group consisting of an anionic polyester having at least one carboxylic group, a sulfonic acid polymer, and a phosphoric acid polymer. A medical device having an antimicrobial composition that includes a complex of an anionic polyester with a monomeric amidoamine having at least one amide group and at least one amine group, wherein the amine group is either a primary amine, or a secondary amine, or a tertiary amine, or a quaternary amine, or a combination thereof and the anionic polyester has at least one carboxylic group is also provided.
WO2013087936A1 Combination of a prostaglandin receptor agonist and an mc1r receptor agonist for the treatment and/or prevention of pigmentation disorders The invention relates to a combination of compounds for the treatment and/or prevention of skin conditions linked to hypopigmentation. It is characterized by a combination product comprising at least one prostaglandin receptor agonist and at least one MC1R receptor agonist, as a medicament for use simultaneously, separately or spread out over time for the treatment and/or prevention of skin conditions linked to hypopigmentation, such as vitiligo.
US20100305167 Administration of an Inhibitor of HDAC Methods of treating patients with SNDX-275 are provided.
US20090149523 Use of n-aminoimidazole cytoprotective compounds for treating cell death and/or gsk-3 mediated diseases The present invention relates to the use of N-aminoimidazole or N-aminoimidazole-thione derivatives as cytoprotective compounds in vitro and in vivo and for the treatment or prevention of cell death mediated disorders and/or GSK-3 mediated disorders or processes.
CN101062031A Method of controlling the quality of silymarin oral aolid preparation The invention discloses an oral solid preparation benefiting for liver with hepadestal as main component, which is characterized by the following: adopting high effective liquid phase method; checking the content of hepadestal; choosing alcohol solution or dilute hydrochloric acid solution as dissolving out medium; testing dissolving degree with ultraviolet spectrophoto method. This invention possesses strong exclusive property and high accuracy, accuracy rating and sensibility.
CN1876151A A pharmaceutical composition for treating cold, its preparation method and use The invention discloses a pharmaceutical composition for treating common cold, which is prepared from dried rehmannia root, honeysuckle flower, curcuma aromatica, capsule of weeping forsythia, patchouli, anemarrhena rhizome, clerodendroa cyrtophyllum, root of ballon flower, licorice root and calcium sulfate. The invention also provides the method for preparation and use of the pharmaceutical composition.
WO2006044228A1 Histamine h3 receptor inhibitors, preparation and therapeutic uses The present invention provides novel compounds with histamine-H3 receptor antagonist or inverse agonist activity. In particular, the invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and intermediates and methods for making these compounds. The invention provides methods of using compounds and pharmaceutical compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
WO2009024585A3 Imidazo [1,2-a] pyrazine compounds for treatment of viral infections such as hepatitis Novel imidazopyrazine compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a viral infection, in particular a HCV, HRV, Sb and/or CVB in a patient in need thereof.
CN103002873A Parenteral pharmaceutical form which releases aromatse inhibitor and gestagens, for the treatment of endometriosis The subject of the present invention for the treatment of endometriosis is the provision of a parenteral pharmaceutical form (release system) for the controlled release of an aromatase inhibitor (AI) with a daily release rate which does not induce any stimulation of the ovaries by negative feedback of the hypophyseal-ovarian axis (which would induce the secretion of gonadotropins and the stimulation of the ovarian follicular growth), and of a gestagen with a daily release rate of below the ovulation-inhibitory dose, which provides a contraceptive effect based on local effects (for example the reduction and thickening of the cervical mucus to prevent the ascent of sperm, effects on the endometrium and on tubal motility in order to hinder the implantation and the transport of ovules).
EP2291380B1 Nalmefene prodrugs The present invention relates to ester prodrugs of nalmefene of formula (I), pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of substance abuse disorders such as alcohol abuse and alcohol dependence and impulse control disorders such as pathological gambling and addiction to shopping.
CN101804024A Gel taking 2beta, 3beta, 12,13-tetrahydroxy-oleanane-28-acid as active component The invention discloses a gel taking 2alpha, 3beta, 12,13-tetrahydroxy-oleanane-28-acid as an active component and also provides a gel composite. The gel composite is characterized by containing the 2beta, 3beta, 12,13-tetrahydroxy-oleanane-28-acid (I) taken as the active component and one or more auxiliary materials used for gel, wherein the content of the 2alpha, 3beta, 12,13-tetrahydroxy-oleanane-28-acid in the gel composite is 0.01-2%.
EP2029097A2 Combination antidepressants wafer The present invention relates to a planar-shaped medication preparation that quickly decomposes on contact with moisture, based on hydrophilic polymers for the release of at least one active ingredient, wherein the medication preparation contains at least one active ingredient combination for treating depression, and with at least one active ingredient selected from the antidepressant group of drugs. The invention also relates to the use of such a combination of active ingredients for the production of an oral medication preparation for the treatment of depression and the therapeutic treatment of depression by means of oral administration of one of the named medication preparations.
WO2013030713A1 Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
WO2012006955A1 Compounds for treatment of metabolic disorders Compounds having activity as agonist of GPR119 and inhibitor of DPPIV are disclosed. These compounds can be used for the treatment and prevention of diseases or conditions in which GPR119 and DPP-IV are involved, selected from diabetes, obesity, impaired glucose tolerance, insulin resistance, diabetic complications, and functional dyspepsia and metabolic diseases caused by abnormal sensitivity to ingested fats in patients.
US20070275949 Benzazepine Derivatives and Methods of Prophylaxis or Treatment of 5Ht2C Receptor Associated Diseases The present invention relates to substituted-2,3,4,5-tetrahydro-3-benzazepine derivatives that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the prophylaxis treatment of 5HT2C receptor associated diseases, conditions or disorders, such as, obesity and related disorders.
US20100093754 Pharmaceutical Compositions Comprising Flibanserin and a Further Agent in the Treatment of Sexual Disorders The invention relates to new pharmaceutical compositions for the treatment of sexual disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient selected from the group consisting of compounds used for female hormone replacement therapy 2a, compounds used for menopause problems 2b, and contraceptives 2c.
EP1534508B1 Embossable and writable multilaminate backing construction A novel backing construction for a transdermal drug delivery system is disclosed. In particular, the invention relates to a system and method for labeling a transdermal drug delivery system, wherein the backing layer contains a writable medium capable of inkless printing.
CN1796377A Antibacterial compound A-40, and application in preparing antibacterial drug This invention publishes an antibacterial compound A-40 with a structural formula (I) and an IUPAC name N-[3-(2-cyclopropionyl-1-benzofuran)]-2-(4-methyl-1-piperdine) acetate, its application in manufacturing antibacterial drugs and its blended composite drugs. This compound, with its pharmacologically permitted ester derivatives, ether derivatives, amino-formyl-N-alkyl derivatives and salts, performs outstanding and broad-spectrum antibacterial activity. It is especially germicidal to leptospiras and some other G- or G+ bacteria and is thus applicable in curing or preventing infection diseases.
WO2012073601A1 Inhibitor of attachment of periodontal-disease-inducing bacterium onto surfaces of teeth, oral biofilm formation inhibitor, and composition for oral applications Provided are: an inhibitor of the attachment of a periodontal-disease-inducing bacterium onto the surfaces of teeth, which has an excellent effect of inhibiting the attachment of the periodontal-disease-inducing bacterium onto the surfaces of teeth; an oral biofilm formation inhibitor which has an excellent effect of inhibiting the attachment of the periodontal-disease-inducing bacterium onto the surfaces of teeth and can exhibit a high biofilm-sterilizing effect; and a composition for oral applications. An inhibitor of the attachment of a periodontal-disease-inducing bacterium onto the surfaces of teeth, which comprises (A) alginic acid propylene glycol ester; an oral biofilm formation inhibitor which comprises (A) alginic acid propylene glycol ester and (B) isopropylmethylphenol; and a composition for oral applications, which is characterized by comprising (A) alginic acid propylene glycol ester and (B) isopropylmethylphenol.
EP2004186A2 Varenicline standards and impurity controls The subject invention provides a varenicline composition that comprises varenicline, or a pharmaceutically acceptable salt thereof, and an amount of a compound selected from one or more of several mononitro, monoamine mixed aminonitro, diamino or dinitro intermediates, and the concentration of said compound is greater than 0 ppm and not greater than about 500 ppm, not greater than about 100 ppm or not greater than about 10 ppm. Methods for synthesizing and using such varenicline compositions are also provided.
WO2010118208A1 Benzoxazepin-4- (5h) -yl derivatives and their use to treat cancer The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
US6929955 Interactive system for presenting and eliminating substances The present invention relates to an interactive system comprising at least one active surface of plastic from monomers containing at least one structural element derived from a carbon dioxide (A), and at least one substance associated to a linker with at least one structural element (B) capable of establishing a hydrogen bond, and involving an interaction between the structural elements (A) and (B). That interactive system is suitable for presenting and eliminating substances in liquids.
WO2012006117A3 Reduction of microglia-mediated neurotoxicity by kca3.1 inhibition Methods for deterring microglia-mediated neurotoxicity in a human or non- human animal subjects comprising the step of inhibiting or blocking the intermediate- conductance calcium-activated potassium channel KCa3.1 in microglia, such as in subjects how suffer from neurodegenerative diseases (e.g., Alzeheimer's Disease) or ischemic/anoxic/hypoxic conditions. The inhibition or blocking of the KCa1.3 channels may be accomplished by administering a KCa3.1 inhibiting substance, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole (TRAM-34).
WO2012074237A2 Liquid medicine composition including dorzolamide and brimonidine for ophthalmology The present invention provides a liquid medicine composition including as active ingredients dorzolamide or a salt thereof, timolol or a salt thereof, and brimonidine or a salt thereof, for ophthalmology, which is stable and non-irritant. More particularly, the present invention provides a liquid medicine composition for ophthalmology comprising: 1-3 w/v% of dorzolamide or the salt thereof; 0.1-1 w/v% of timolol or the salt thereof; 0.1-0.5 w/v% of brimonidine or the salt thereof; 1.0-1.5 w/v% of polyvinylpyrrolidone; 0.2-0.8 w/v% of sodium chloride; 0.3-0.6 w/v% of a buffering agent; a preservative; a pH controlling agent; and water.
CN101406462A Domperidone orally disintegrating tablets as well as preparation method and quality control method thereof The invention discloses a domperidone oral disintegrating tablet, and a method for preparing the same and a method for quality control. The domperidone oral disintegrating tablet is prepared from domperidone and auxiliary materials, and the quality thereof is controllable and stable. The domperidone oral disintegrating tablet is a peripheral dopamine receptor agonist which is safe and effective. Compared with the prior art, the domperidone oral disintegrating tablet has the advantages of rapid disintegration, convenient taking, no vomiting, rapid effect, and low side effect.
US7141691 Derivatives of carboplatin with fewer undesired side-effects and higher efficacy towards tumor tissue; for treatment of cancer The invention concerns low-molecular platinum complexes containing cyclobutane-1,1-dicarboxylate ligands that contain a protein-binding group.
CN101648008B Compound preparation used for joint care and preparation method thereof The invention discloses a compound preparation used for joint care and a preparation method thereof. The compound preparation comprises active ingredients and auxiliary materials, wherein the active ingredients comprise glucosamine, chondroitin sulfate, dimethyl sulfone and collagen, and the glucosamine is glucosamine sulfate or glucosamine hydrochloride or glucosamine phosphate or mixture of theglucosamine sulfate and the glucosamine hydrochloride and the glucosamine phosphate; and the auxiliary materials comprise excipient, disintegrant, lubricant, bonding agent and wetting agent. The invention has better treatment and prevention functions on arthritis and joint injury; the prepared tablet has good disintegration property, rapid digestion, quick effect taking, strengthened stability and high absorption and utilization ratio; and the consumption of the raw materials and the auxiliary materials achieves the optimal proportion.
WO2005000406A3 Treatment of amyloid- and epileptogenesis-associated diseases Methods of treating or preventing an amyloid-related disease in a subject by administering to a subject a therapeutic amount of a compound of the invention are described. Also included are methods for inhibiting epileptogenesis in a subject, by administering to a subject an effective amount of an anti-epileptogenic agent. Methods for treating a subject suffering from an epileptogenesis-associated condition, by administering to the subject an effective amount of an anti-epileptogenic agent are also included. Methods for treating convulsions in a subject by administering to the subject an effective amount of a therapeutic amount of a compound of the invention are also described.
CN1989960A Andrographolide dispersed tablet The invention involves andrographolide disintegrating tablet. The invention drugs uses the andrographolide as raw materials, prepares fines of andrographolide extract, adds suitable findings to making andrographolide disintegrating tablet which can collapse completely in 3 minutes and distributes uniformly, and the invention has the effects of heat clearing, detoxicating, antibiosis and anti-inflammation. It can be used for upper respiratory tract infection and bacillary dysentery. The disintegrating tablet can collapse rapid when in water to dissolving into fragrance and sweet solution, so it is easier for patients to accepting and using, and more convenient for bring and use and other features. The preferred findings in the invention can make andrographolide disintegrating tablet collapse more rapidly.
WO2007072902A1 Therapeutic agent for acute cerebral infarct Disclosed is a therapeutic agent for acute cerebral infarct which comprises (2R)-2-propyloctanoic acid or a salt thereof and is intended to be administered about 5-72 hours after the onset of symptoms. The therapeutic agent is safe and can ameliorate acute cerebral infarct or various conditions accompanied by acute cerebral infarct in a patient suffering from cerebral infarct, particularly a patient suffering from cerebral infarct who shows a score of 22 or smaller as measured according to NIH stroke scale, and therefore the therapeutic agent is useful for the treatment of acute cerebral infarct.
CN103520092A Monocrotaline gel and preparation method thereof The invention provides a monocrotaline gel and a preparation method thereof, belonging to the technical field of monocrotaline preparations. Each kg of the gel comprises 1.2 g of monocrotaline, 5 to 10 g of carbomer-940, 50 to 150 ml of glycerin, 10 to 50 ml of azone, 200 to 300 ml of absolute ethyl alcohol and 5 to 10 g of methylparaben, with the balance being distilled water, and triethanolamine is used to adjust a pH value to neutral. According to the invention, the gel is prepared from monocrotaline and used for treating squamous-cell carcinoma, and the gel can avoid toxic and side effects on the whole body caused by oral administration or intravenous injection and intramuscular injection and achieves the purposes of local treatment of diseases and improvement of living quality of patients; furthermore, through single factor investigation and orthogonal design, accessories for the gel are screened, which enables monocrotaline to be more stable and to better perform its effects.
US20100104614 Providone compositions for wound healing Described here are wound dressings and kits. The wound dressings include povidone compositions that may be directly applied to wound surfaces or provided on substrates to form a composite material. The povidone compositions contain a povidone polymer, where the povidone polymer itself is capable of healing wounds. The povidone compositions may be in particulate form. In other instances, the povidone compositions are formulated as gels, ointments, pastes, films, or other topically applied compositions. Methods for applying the povidone compositions to treat wounds are also described.
CN101559073A Cordyceps and ganoderma lucidum polysaccharides compound preparation with immune synergism The invention provides a cordyceps and ganoderma lucidum polysaccharides compound preparation with immune synergism, which is a compound preparation consisting of polysaccharides from cordyceps and ganoderma lucidum polysaccharides. Dosage forms prepared from the polysaccharides compound have the immunoregulation function, can obviously improve the activity of NK cells, the phagocytic activity of macrophage of organisms, and cellular immunity and humoral immunity functions of the organisms, and have immunoregulation function on the organisms. The cordyceps and ganoderma lucidum polysaccharides compound preparation solves the problem that active ingredients cannot take effect fully because cordyceps, and mycelium or encarpium of ganoderma are directly used as medicaments.
WO2013038395A1 Transition metal complexes for pharmaceutical applications The family of ruthenium compounds that is subject of the present patent was found to exhibit great potential as pharmaceutical agents for the treatment of cancer condition. In fact, the present compounds which structure is based on piano stool Μ(η5- ciclopentadienyl ) (M=Ru, Fe) possessing compulsory sigma bonded heteroaromatic ligands to treat tumor and /or metastasis. These compounds displayed very high efficiency in vitro in what concerns their cytotoxicity against a wide range of tumor cells significantly surpassing the activity of the benchmark metallodrug cisplatin currently in clinical use. In addition, we have identified biological targets involved in th mode of action of the ruthenium compounds such as, PARP-1 (a Poly- (adenosine diphosphate (ADP) -ribose) polymerase enzyme) and cell regulatory proteins (cytochrome C and ubiquitin). Although DNA is not the main target of the ruthenium compounds, their interaction with DNA was proved by different approaches. These agents bind to albumin which can provide a vehicle for their transport in the blood stream without loss of activity. Overall this family of compounds encloses a panel of highly promising new anti-tumor ruthenium agents with a large spectrum of activity.
WO2008023283A3 Stabilized esters of lutein The invention describes lipoic acid or dihydrolipoic acid esters of xanthophylls, such as lutein, that have improved stability and bioavailablity versus simple mixtures of lipoic or dihydrolipoic acid and the xanthophyll.
CN101506162A Substituted isoindoles as bace inhibitors and their use This invention relates to novel compounds having the structural formula I and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
US20060084595 Complex comprising OCIF and polysaccharide A complex comprising at least one substance selected from the group consisting of an osteoclastogenesis inhibitory factor, an analogue thereof and a variant thereof, which is bound to at least one substance selected from the group consisting of a polysaccharide and a polysaccharide derivative. The complex has a prolonged retention in the bloodstream after administration, making it useful in the treatment and prophylaxis of bone metabolic diseases.
CN102731580A Binuclear platinum (II)-diphosphonic acid coordination compound, preparation method and application thereof The invention provides a binuclear platinum (II)-diphosphonic acid coordination compound, a preparation method and an application thereof, and belongs to the field of anti-cancer drugs. The binuclear platinum (II)-diphosphonic acid coordination compound has the structural formula shown in the description, wherein n is 2, 3, 4 or 5. The preparation method of the binuclear platinum (II)-diphosphonic acid coordination compound comprises the following steps: diphosphonic acid derivative and Pt(en)(OSO3)(H2O) are reacted under the function of Ba(OH)2 to obtain the binuclear platinum (II)-diphosphonic acid coordination compound. According to the compound, a link arm of C between diphosphonates is expanded; quinary aromatic amine (namely imidazole) is introduced in, so that at the initial usage stage of the coordination compound, the coordination compound has high intake in tumour cells and long residence time; and the aggregation concentration of the coordination compound in other non-targeted tissues is greatly reduced.
CN101219133A Levorotation carnitine pellet and method for preparing the same The invention provides a levocarnitine micro-pill which is prepared from levocarnitine and pharmaceutic adjuvant, characterized in that the pharmaceutic adjuvant is an excipient and a bonding agent; the content of the levocarnitine in the levocarnitine micro-pill is 10 to 90 weight percent; the excipient 20-80 weight percent and the bonding agent 1-5 weight percent. The levocarnitine micro-pill of the invention has the advantages of high dissolution rate, high bioavailability, easy preparation method and convenient and easy operation.
CN102178653B Aclacinomycin nanometer grain and preparation method thereof The invention discloses an aclacinomycin nanometer grain and a preparation method thereof. The aclacinomycin nanometer grain is not attached to a carrier material and is directly applied to ensure that the drug dosage can be increased, the toxicity and the side effect which are caused by the carrier can be eliminated and the treatment effect can be improved; in the preparation method, a low-boiling-point organic solvent is combined with an emulsification technology and process to directly prepare the aclacinomycin (comprising aclacinomycin A and aclacinomycin B) nanometer grain without the carrier material; and the aclacinomycin nanometer grain prepared by utilizing the preparation method provided by the invention has a spherical appearance and a rounding and smooth surface, and the grainsize is in a range of 10-1000nm.
CN101933992A Powder for treating oral ulcer The invention relates to powder for treating oral ulcer. The powder is prepared from the following raw materials in part by weight: 3 to 8 parts of medicinal cyathula root, 4 to 8 parts of tangerine peel, 3 to 6 parts of Chinese angelica, 2 to 5 parts of bupleurum, 3 to 6 parts of Chinese magnoliavine fruit, 0.1 to 1 part of borneol, 3 to 6 parts of chicken's gizzard-membrane, 2 to 6 parts of szechuan lovage rhizome, 1 to 4 parts of alum, 3 to 7 parts of liquoric root and 2 to 6 parts of angelica dahurlica. The powder of the invention has the advantages of having relatively obvious treatment effect for patients suffering from serious recurrent oral ulcer for a long time, fully improving immunologic function, enhancing the body resistance, killing ulcer viruses, curing ulcer and avoiding or eliminating recurrence for a relatively long time, along with simple composition, low cost and relatively ideal treatment effect.
US20090181919 Method for Freeze-Drying Nucleic Acid/Block Copolymer/Cationic Surfactant Complexes This invention relates generally to the freeze-drying of formulations comprising a polynucleotide, a block copolymer and a cationic surfactant. In the presence of a cryoprotectant or bulking agent, a formulation can be freeze-dried, whereby upon reconstitution of the dried formulation, the microparticles maintain their optimal size and aggregation or fusion is avoided.
CN102973875A Medicament for strengthening spleen, checking diarrhea and removing food retention for children The invention relates to a medicament for strengthening the spleen, checking diarrhea and removing food retention for children. The medicament is prepared from the following raw medicines in parts by weight: 1-20 parts of parched hawthorn fruit, 1-20 parts of endothelium corneum gigeriae galli, 1-20 parts of fructus amomi, 1-40 parts of betel nut, 1-20 parts of trogopterus dung, 1-40 parts of red halloysite, 1-30 parts of lotus leaves, 1-40 parts of semen plantaginis and 10-80 parts of isatis roots. The medicament used for strengthening the spleen, checking diarrhea and removing food retention for children has an appropriate formula and can be effectively used for strengthening spleen, checking diarrhea and removing food retention for children.
WO2008146731A1 Method for preparation of infusion solution for peripheral intravenous administration The object is to produce an infusion solution for peripheral intravenous administration which comprises a sugar solution containing vitamin B1 and an amino acid solution, both of which are contained separately in chambers in a communicatably constituted multi-chamber container, in such a manner that the degradation of an amino acid can be reduced. Specifically disclosed is a method for producing an infusion solution for peripheral intravenous administration, which comprises a sugar solution containing a sugar, a portion of an electrolyte and vitamin B1 and an amino acid solution containing an amino acid, a portion of the electrolyte and a sulfite salt, both of which are contained separately in chambers in a communicatably constituted multi-chamber container. In the method, a carbon dioxide gas is dissolved in the amino acid solution to adjust the pH value of the amino acid solution to a neutral value prior to the high-temperature sterilization of the amino acid solution, sterilizing the solution at a high temperature, and packaging the solution together with an iron-containing deoxygenating agent with a non-gas-permeable outer packaging material having a light-shielding property.
US6987092 Indigoid bisindole derivatives The present invention relates to novel indigoid binsindole derivatives which can be used for the manufacture of a medicament for the treatment of solid cancers.
WO2009071905A3 Use of thiolatocobalamins as regulators/selective promoters of inducible and constitutive nitric oxide synthases The present invention provides methods of treatment and uses of thiolatocobalamin compounds for diseases characterised by NOS depression, malfunction, or dysregulation, for example inflammation, the inflammatory phase of the immune response, SIRS/sepsis/septic, traumatic, anaphylactic shock, a bacterial, viral or parasitidal disease, cancer, spinal injury or cardiovascular disease.
US20070249720 Thiourea Derivative-Containing Pharmaceutical Composition Having Improved Solubility and Bioavailability The present invention relates to a pharmaceutical composition comprising a thiourea derivative or its pharmaceutically acceptable salt, a cyclodextrin or its derivative; and a pharmaceutical formulation comprising same.
CN103156830A Application of aloe-emodin in resisting SARS coronavirus infection The invention provides an application of aloe-emodin in preparing drugs for preventing and trating SARS coronavirus infection, and particularly relates to an application in preparing SARS coronavirus main protease inhibitors. The aloe-emodin has the following structural formula. The aloe-emodin has the effect for inhibiting the activity of SARS coronavirus main protease, and an IC50 value of the aloe-emodin is 95 [mu]m.
US20110200557 New 2-amidothiadiazole derivatives The present disclosure relates to 2-amidothiadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.
CN101333525A SiRNA sequence against HCMV UL86 gene and applications The invention provides a cDNA sequence of siRNA aiming at a cytomegalovirus UL86 gene of human, and the nucleotide sequence is: 5`-GCACGTCAGTTATCATCAACA-3`. According to the design principle of the siRNA, the cDNA sequence of the selected siRNA has a GC content of 42.9 percent, and the selected siRNA is corresponding to 3161-3181 nucleotide sites in UL86 mRNA, siRNA eukaryotic expression vectors aiming at the HCMV UL86 gene are constructed, and plasmids are extracted after transforming Escherichia coli for transfecting AD293 cells, thereby effectively inhibiting the UL86 gene mRNA and the protein expression level, and the sequence can be applied to the preparation of drugs for curing cytomegalovirus infection of human.
WO2011034920A1 Compositions and methods for treating seizure disorders Disclosed are methods of treating a seizure disorder by administering to a patient in need of such treatment a compound having the following formula (I).
CA2229960C Steroid compounds having contraceptive and anti-osteoporosis activity The invention relates to a steroid compound having the formula (I) see formula(I) comprising a ring E, said ring sharing carbon atoms at position 16 and 17 with the five-membered ring D and being a with respect to said D-ring. In addition, the carbon atom at position 17 is substituted with an oxygen atom-comprising group through a CO bond. The invention also relates to a pharmaceutical composition comprising said steroid compound. The steroid compounds of the present invention are very suitable for use in the prevention or treatment of peri-menopausal or menopausal complaints, more preferably the prevention or treatment of osteoporosis. Furthermore, the steroid compounds of the present invention can be used for contraceptive purposes.
US20090016991 Rxr Antagonist Treatment Against Multiple Sclerosis Retinoids with retinoid antagonistic activities, especially Retinoid X Receptor antagonists called RXR antagonists, pharmaceutically acceptable salts and pharmaceutically acceptable esters and amides thereof, have been found to be effective in the treatment of multiple sclerosis, especially by systemic such as oral administration of RXR antagonists.
US20100311690 Boropeptide inhibitors of enteropeptidase and their uses in treatment of obesity, overweight and/or diseases associated with an abnormal fat metabolism The present invention relates to novel compounds, particularly derivatives of boroarginine, boroornithine and borolysine that selectively modulate, regulate, and/or inhibit enteropeptidase. The invention also relates to compositions, particularly pharmaceutical compositions, as well as methods to treat excess weight, obesity and diseases associated with an abnormal fat metabolism.
WO2011140160A1 Bicyclic heteroaryl compounds as gpr119 modulators Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein- coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
CN103520100A Etoposide self-microemulsion preparation as well as preparation method and application thereof The invention relates to an etoposide self-microemulsion preparation as well as a preparation method and application thereof, and belongs to the technical field of medicine. An etoposide self-microemulsion is prepared by taking etoposide as a medicinal active ingredient through cooperating a suitable emulsifier, an auxiliary emulsifier and a stabilizer.
WO2013092753A1 Indole derivatives inhibitors of enzyme lactate dehydrogenase (ldh) The present invention encompasses compounds having general formula (I) able to inhibit the lactate production (lactic acid) involved in the angiogenesis of tumoral tissues, in the glycolytic metabolic process of tumoral cells, of immune system cells in asthmatic diseases, in vascular cells in the pulmonary hypertension, in the treatment of chronic back pain or hyperoxaluria, and in the process by which the parasites protozoan causing malaria obtain most of the necessary energy
US20110003823 Compositions and methods for treatment of diseases and conditions associated with vasodilation and/or vascular leakage The invention provides compositions and methods for treating diseases and conditions, including systemic diseases and conditions, through an intravenous administration of a selective α-2 adrenergic receptor agonists having a binding affinity of 300 fold or greater for α-2 over α-1 adrenergic receptors. The amounts of the selective α-2 adrenergic receptor agonists are substantially lower than the amounts normally used to cause sedation. The compositions preferably include dexmedetomidine.
WO2013106570A1 Combination of beta-hydroxy-beta-methylbutyrate, arginine and glutamine for use in treating diabetic ulcers Disclosed is the combination of beta-hydroxy-beta-methylbutryate, arginine, and glutamine for use in a method of treating a diabetic ulcer in a diabetic individual having at least one of: (a) a serum albumin level of less than or equal to 4.0 g/dL, and/or (b) an Ankle-Brachial Index of less than 1.0. 9. Also disclosed is the use of the combination of beta-hydroxy-beta-methylbutryate, arginine, and glutamine for the manufacture of a medicament for use in the treatment of a diabetic ulcer in a diabetic individual having at least one of: (a) a serum albumin level of less than or equal to 4.0 g/dL, and/or (b) an Ankle-Brachial Index of less than 1.0. In certain embodiments, the combination of beta-hydroxy-beta-methylbutyrate, arginine, and glutamine are orally administered via a nutritional composition.
EP2482815A1 Anti inflammatory 2-oxothiazoles and 2 -oxooxazoles A compound of formula (I) wherein X is O or S; R1 is H, OH, SH, nitro, NH2, NHC1-6alkyl, N(C1-6alkyl)2, halo, haloC1-6alkyl, CN, C1-6-alkyl, OC1-6alkyl, C1-6alkylCOOH, C1-6alkylCOOC1-6alkyl, C2-6-alkenyl, C3-10cycloalkyl, C6-10aryl, C1-6alkylC6-10aryl, heterocyclyl, heteroaryl, CONH2, CONHC1-6alkyl, CON(C1-6alkyl)2, OCOC1-6alkyl, or is an acidic group, such as a group comprising a carboxyl, phosphate, phosphinate, sulfate, sulfonate, or tetrazolyl group; R2 is as defined for R1 or R1 and R2 taken together can form a 6-membered aromatic ring optionally substituted by up to 4 groups R5; R3 is H, halo (preferably fluoro), or CHaI3 (preferably CF3); each R5 is defined as for R1; V1 is a covalent bond or a C1-20alkyl group, or C2-20-mono or multiply unsaturated alkenyl group; said alkyl or alkenyl groups being optionally interupted by one or more heteroatoms selected from O, NH, N(C1-6alkyl), S, SO, or SO2; M1 is absent or is a C5-10 cyclic group or a C5-15 aromatic group; and R4 is H, halo, OH, CN, nitro, NH2, NHC1-6alkyl, N(C1-6alkyl)2, haloC1-6alkyl, a C1-20alkyl group, or C2-20-mono or multiply unsaturated alkenyl group, said C1-20alkyl or C2-20alkenyl groups being optionally interupted by one or more heteroatoms selected from O, NH, N(C1-6 alkyl), S, SO, or SO2; with the proviso that the group V1M1R4 as a whole provides at least 4 backbone atoms from the C(R3) group; or a salt, ester, solvate, N-oxide, or prodrug thereof; for use in the treatment of a chronic inflammatory condition.
US20050009902 Treating any types of pruritus such as ocular pruritus, skin pruritus and systemic pruritus with a cannabinoid agonist such as palmidrol and anandamide or a derivative The invention aims to find out a novel pharmacological effect (medical use) of cannabinoid. Since cannabinoid agonists such as palmidrol and anandamide have an excellent antipruritic effect, they are useful as an agent for treating any types of pruritus such as ocular pruritus, skin pruritus and systemic pruritus.
WO2007142309A1 Method of screening drug for treating kidney glomerulus A method of screening a compound usable in preventing, relieving or treating a kidney glomerular lesion characterized by comprising examining a test compound with respect to its controlling effect on the expression of 4F2hc which is induced by contacting a cultured human cell line having the properties of human peripheral mononuclear cells, human mononuclear cells or human macrophages with a macrophage activator. This screening method is useful in screening a compound which is usable in preventing, relieving or treating a kidney glomerular lesion.
US20120141384 Antibacterial conjugated boronic acids and pharmaceutical compositions thereof A method of treating a disorder associated with a bacterial infection, consisting of administrating a pharmaceutical composition, comprising (a) a therapeutically effective amount of a conjugated boronic acid or a derivative thereof; and (b) a suitable pharmaceutical vehicle. The invention further relates to suitable pharmaceutical vehicles and pharmaceutical compositions for treating such disorders.
CN102000032B Method for preparing ketoprofen slow release preparation The invention belongs to the field of medicines, and particularly relates to a method for preparing a ketoprofen slow release preparation. The method for preparing the ketoprofen slow release preparation realizes steady blood concentration after administration and can also realize the purpose of steadily releasing ketoprofen within 24h. The ketoprofen slow release preparation mainly comprises thefollowing components in parts by weight: 200 parts of ketoprofen and 110-120 parts of slow release skeleton matrix, wherein the ketoprofen is used as a main ingredient, and the slow release skeleton matrix consists of hydroxymethyl propyl cellulose K4M and hydroxymethyl propyl cellulose K100M in the ratio of 5: 1. The method for preparing the ketoprofen slow release preparation comprises the following steps of: A, mixing the ketoprofen and the slow release skeleton matrix; and B, adding pharmaceutically-acceptable accessories to prepare the slow release preparation. By applying the ketoprofenslow release preparation, long-acting slow release is realized, the peak value and the valley value of blood concentration are reduced, the blood concentration is more steady, the half-life period iseliminated up to 11h; and the ketoprofen slow release preparation can especially satisfy steady release within 24h and just needs to be taken once a day.
US7163929 Methods and compositions for treating flaviviruses and pestiviruses A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
EP2556069A1 Pyrimidinylpiperidinyloxypyridinone analogues as gpr119 modulators Novel compounds of structure Formula (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein n1, R1, R2, R3 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
CN101658494B Huperzine A solid lipid nano particle and preparation method thereof The invention relates to the field of pharmaceutical preparations, which discloses a huperzine A solid lipid nano particle and a preparation method thereof. The huperzine A solid lipid nano particle is prepared from the following components in weight percent: 0.05-1% of huperzine A, 3-10% of lipid material, 2-10% of emulsifying agent and the balance water. The preparation method adopts a high-pressure even emulsification method to coat the huperzine A into a solid lipid nano particle so as to prepare the huperzine A solid lipid nano particle. The particle diameter of the huperzine A solid lipid nano particle prepared by the invention is 10-100nm, the medicine envelopment rate and the medicine-carrying quantity are high, and the stability is good; simultaneously, the use of an addition agent and an organic solvent which are harmful to a human body is avoided; and the bioavailability is enhanced, the brain targeting property is increased, and the dose and the toxic or side effect are small.
US20120142725 Combined Use of an Alpha-Adrenergic Receptor Antagonist and an Anti-Muscarinic Agent The combined use of (R)-5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzene-1-sulfonamide (tamsulosin), or its pharmaceutically acceptable salt, and (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylic acid (3R)-quinuclidin-3-yl ester (solifenacin), or its pharmaceutically acceptable salt, for the preparation Of a medicament for the improvement of lower urinary tract symptoms associated with benign prostatic hyperplasia (LUTS/BPH) with a substantial storage component is provided.
US7105501 Compositions with vascular damaging activity Compositions for the inhibition of the formation of new vaculature by angiogenesis are provided as in compounds which are salts comprising as an acidic component a compound of formula (1) wherein: R1, R2 and R3 are each independently alkyl, R4 is alkoxy, haloalkoxy, alkyl, haloalkyl, alkenyl, alkynyl, alkylthio, alkylsulphinyl, alkylsulphonyl, hydroxy or halo, R5 is hydrogen, alkoxy, alkyl, alkylthio, hydroxy, phosphate or halo, and, as the basic component, a compound selected from the group consisting of (2) a compound of formula (2) wherein R6 is hydrogen or alkyl R7 is alkyl, alkylamino, dialkylamino, nitroamino, hydrazine, mercapto or alkylthio X is CH2, CH2CH2, CH2S, CH2CH2S Y is NH or S or a compound of formula (3) wherein R8 is alkyl or aminoalkyl R9 is hydrogen, alkyl or optionally substituted phenyl or, a compound of formula (4) wherein Z is O, S, CH2, CHR13 or a bond R10, R11, R12 and R13 are each independently alkyl or hydrogen or, a compound of formula (5) wherein R14 is alkyl and the pharmaceutically acceptable solvates and hydrates thereof.
US20110123654 Synergistic enhancement of cellular ergogenic nutrient uptake, like creatine or carnitine, with tarragon A product comprising a) Russian Tarragon (Artemisia dracunculus), an extract of Russian Tarragon or a derivative thereof b) a creatine and/or carnitine compound or derivative or precursor thereof.
WO2011113368A1 Preparation method of fluoro-substituted deuterated diphenylurea A fluoro-substituted deuterated diphenylurea compound, especially 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)- 2-(N-1',1',1'-d3-methyl)picolinamide, preparing method and use for treating or preventing tumor and relative diseases thereof.
EP1758591B1 Invert emulsion composition containing calcitriol and clobetasol 17-propionate, and uses thereof in cosmetics and dermatology The invention concerns a composition containing two active principles, namely calcitriol and clobetasol 17-propionate, and uses thereof in cosmetics and dermatology, as well as a method for preparing same. The invention is characterized in that the composition is an invert emulsion containing a hydrophilic glycolic or hydroglycolic dispersed phase, a continuous lipophilic phase and an emulsifier with hydrophilic-lipophilic balance (HLB) ranging between 2 and 7.
CN102188384A Microsphere preparation method for adjusting and controlling release behavior of risperidone microspheres and for controlling size thereof The invention relates to a microsphere preparation method for adjusting and controlling the release behavior of risperidone microspheres and for controlling the size thereof, belonging to the technical field of nano-medicaments. The preparation method comprises the steps of: firstly, adding a sustained-release or controlled-release functional material to one or the mixture of dichloromethane, ethyl acetate and acetonitrile, swirling and dissolving to obtain an organic solution of the sustained-release or controlled-release functional material; then adding particles containing risperidone and an alkaline matter to the organic solution of the sustained-release or controlled-release functional material, i.e. stirring or swirling in the oil phase to evenly disperse to form even suspension; and adding the suspension to SPG (Shirasu Porous Glass) membrane emulsion with different bore diameters, enabling the suspension to enter brine containing a surfactant through the membrane emulsion by adjusting the pressure, stirring to form microspheres, and transferring into the brine for solidifying to finish preparation. The biodegradable risperidone microsphere sustained-release preparation prepared by the invention has quick effect taking speed and long drug release time, the particle size of the microspheres is controllable, the envelop rate is high, and the quality of the risperidone microspheres is controllable.
US20120252795 Oral lysophilisates containing pvp/va The present invention relates to novel oral pharmaceutical compositions in lyophilized form, in which the dissolution and the bioavailability of the active ingredient that they contain are improved. The compositions according to the invention comprise in particular a polyvinyl acetate/polyvinylpyrrolidone copolymer. The oral lyophilisates according to the invention are particularly suitable for the production of medicaments based on active ingredients which have low solubility or very low solubility in water or which are virtually insoluble in water.
US20060160754 Glycyrrhizin high-concentration preparation To provide a glycyrrhizin/aminoacetic acid/cysteine combination drug containing an active ingredient in high concentration and excelling in stability and safety. Stability at compounding of active ingredient in high concentration has been improved by avoiding the addition of sulfite salts having been used as a stabilizer in existing products. As glycyrrhizin high-concentration preparations, there is provided a drug composition comprising 8 to 16 mg/mL of glycyrrhizin, 3 to 6 mg/mL of cysteine and 80 to 160 mg/mL of aminoacetic acid wherein no sulfite salts are added as an additive.
WO2014052619A1 Piperidine derivatives and compositions as modulators of gpr119 activity The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. The compounds are of Formula I: wherein the variables are as defined herein.
CN103316036A Pure natural artificial tear and its preparation method The invention relates to an artificial tear, especially to a pure natural artificial tear and its preparation method. The pure natural artificial tear is composed of 4-8 wt% of a salt lake saturated brine aqueous solution, wherein the content of sodium chloride in the salt lake saturated brine is 0.4-1.6 wt%. The preparation method of the pure natural artificial tear comprises the following preparation steps: removal of sodium chloride, refining of salt lake brine and dilution. The technical scheme provided by the invention has characteristics of obvious treatment effect, no side-effect, wide sources of raw materials, simple preparation technology, low treatment cost, simple usage and the like. By the use of the pure natural artificial tear, dry eye syndrome which has high morbidity at present can be effectively treated.
CN101268048A Carbazole derivatives Disclosed are compounds and pharmaceutically acceptable salts of Formula I: wherein n, R1, R2, R3, X, R4, R5, R6, R8, R9, and Y are as Defined herein. Compounds of Formula I am useful in the treatment of diseases and/or conditions related to cell proliferation and/or abnormal cell mitosis, such as cancer, inflammation and inflammation-associated disorders, and conditions associated with angiogenesis. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
CN101181579B Chrysanthemum row containing natural aromatic plant The invention relates to a chrysanthemums medicine strip which contains natural fragrant plants, and comprises 80 to 85 parts of chrysanthemum, 5 to 10 parts of wild chrysanthemum, 5 to 10 parts of honeysuckle, 2 parts of fructus amomi, 2 parts of banksian rose and 2 parts of sodium carboxymethyl cellulose. The invention is a composite, wherein, the chrysanthemum has the effects of dispersing wind-heat, calming liver and improving eyesight due to the rich vitamin A contained in the chrysanthemums; the wild chrysanthemum has effects of clearing away heat and toxic materials, and has obvious curative effect on red eyes, sore throat, headache and dizziness; the honeysuckle has effects of clearing away heat and toxic materials; the fructus amomi has the effects of eliminating dampness, dispelling cold, expelling phlegm and preventing recurrence of malaria; and the banksian rose has the effects of promoting circulation of qi and relieving pain. In addition, when matched with the well-knownadjustable needle warming moxibustion apparatus, the invention can realize safe health regulation, health care physical therapy and skin-beautifying upkeep for people, and has the advantages of obvious physical therapy effect, delightful fragrance and low cost.
WO2013143184A1 Streptomyces, and anti-tumor compounds spiro-indimycin a-d and preparation method and application thereof Provided is a streptomyces (Streptomyces sp.) strain SCSIO 03032, preserved in China Center for Type Culture Collection on July 18, 2011 with the preservation number CCTCC NO: M 2011258. The streptomyces (Streptomyces sp.) strain SCSIO 03032 can be used to produce compounds Spiro-Indimycin A, B, C and D with antineoplastic activity; the compounds not only have a rare spiral structure, but also have selectivity and highly-efficient activity for tumour cells. Further provided are a preparation method and an application of the compounds Spiro-Indimycin A, B, C and D.
US7195902 Expression vector comprising nucleotide sequences coding JNK activating phosphatase for use identifying modulator for treatment of inflammatory, arthritic, cardiovascular, respiratory cell proliferative and liver disorders The present invention provides novel JNK activating phosphatase polypeptides and nucleic acid molecules encoding the same. The invention also provides vectors, host cells, antibodies and methods for producing JNK activating phosphatase polypeptides. Also provided for are methods for the diagnosis and treatment of diseases associated with JNK activating phosphatase polypeptides.
EP2361922A1 Intermediate to HCV-Nucleoside Inhibitors A compound having the formula: which is of use in the preparation of HCV-nucleoside inhibitors.
CN103450113A Thiadiazine-triketones-substituted derivative, preparation method thereof and application As is shown in a general formula I, the invention discloses a thiadiazine-triketones-substituted derivative, salt, ester or prodrug acceptable in pharmacy, a preparation method of the derivative, and application of a combination containing one or more compounds of the similar type in drugs treating and preventing human immunodeficiency virus (HIV) infection.
WO2012045194A1 Benzodiazepinones as fak inhibitors for treatment of cancer Disclosed are compounds which inhibit the activity of focal adhesion kinase, compositions containing the compounds, and methods of treating diseases during which focal adhesion kinase is expressed.
US20090062403 Compositions and Methods for Treatment of Disorders of Protein Aggregation The invention provides compositions, methods and uses comprising a scyllo-inositol compound that provide beneficial effects in the treatment of a disorder and/or disease including a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence.
WO2007058894A3 Splice switching oligomers for tnf superfamily receptors and their use in treatment of disease Methods and compositions are disclosed for controlling expression of TNF receptors (TNFRl and TNFR2) and of other receptors in the TNFR superfamily using compounds that modulate splicing of pre-mRNA encoding these receptors. More specifically these compounds cause the removal of the transmembrane domains of these receptors and produce soluble forms of the receptor which act as an antagonist to reduce TNF-α activity or activity of the relevant ligand. Reducing TNF-α activity provides a method of treating or ameliorating inflammatory diseases or conditions associated with TNF-α activity. Similarly, diseases associated with other ligands can be treated in like manner. In particular, the compounds of the invention are splice-splice switching oligomers (SSOs) which are small molecules that are stable in vivo, hybridize to the RNA in a sequence specific manner and, in conjunction with their target, are not degraded by RNAse H.
US20090029957 8-beta-substituted estratrienes as selectively active estrogens The invention refers to 8β-substituted estra-1,3,5(10)-triene derivatives of general formula I their use as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action in the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.
US20090176773 Non-Peptidic Inhibitors of AKAP/PKA Interaction The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.
WO2012078519A2 3-acylidene-2-oxoindole derivatives for inhibition of transglutaminase 2 Provided herein are acylidene oxoindole derivatives, compositions including them, and methods of inhibiting transglutaminase 2 and treating diseases mediated by transglutaminase 2 by administering such derivatives and compositions.
CN101003490A Chelated silver amino nitrate, preparation method and application This invention relates to preparation and application of nitric acid and amino acid chelated silver compound. The compound is prepared from amino and carboxyl-containing compounds and AgO. Experiments show that the compound can be widely applied in medicine, antibacterial materials, silver coating, photosensitive materials, fresh preservation materials and reagents.
WO2013111714A1 Prophylactic or therapeutic agent for bronchial asthma and method for screening same The present invention provides a prophylactic or therapeutic agent for bronchial asthma, said agent comprising a heme peroxidase inhibitor. Thus, a prophylactic or therapeutic agent for bronchial asthma, which has a function mechanism different from the function mechanism of inhaled steroids and is usable as a substitute for inhaled steroids, is provided.
US7255882 Enkephalinase inhibitor and GABA precursor loading as anti-anxiety compositions Benzodiazepine withdrawal induced anxiety is treated by administration of an enkephalinase inhibitor, and a gamma-aminobutyric acid (“GABA”) precursor, or an endorphin or enkephalin releaser. These components promote restoration of normal neurotransmitter function and are non-addictive. Use of the enkephalinase inhibitor D-phenylalanine, the GABA precursor glutamine, the serotonin precursor 5-HTP, glycine, and taurine, in combination with coenzymatic functionality of folic acid is preferred for activation of ligand-gated Cl− channel in the central nervous system. Food supplement embodiments provide the human body nutritional supplements to intake certain neurotransmitter precursor substrates, thereby enabling patients of all ages to self-regulate their ability to quell perturbations to equilibrium and simultaneously to adverse effects upon normal physiological and psychological functioning attributable to induced anxiety and panic associated with benzodiazepine withdrawal.
US20100249116 Compositions and Methods for Treating Intoxications Compositions and methods for treating intoxication by poisonous agents are described. In one aspect the pharmaceutical compositions include a phenothiazine compound, a dioic acid compound and a pharmaceutically acceptable carrier. In another aspect the pharmaceutical composition can include a phenothiazine compound, a nitroester compound, ethanol and a pharmaceutically acceptable carrier.
CN1872043A Application of salvianolic acid B in preparing medication for preventing tumorigenesis An application of danshinolic acid in preparing the medicines in the form of tablet, oral liquid, injection, spray, or suppository for preventing tumor is disclosed.
CA2141056C Treatment of dentoalveolar infections with taurolidine and/or taurultam The present invention provides a new means of combatting severe dentoalveolar infections such as dental gangrene, parodontitis and abscesses which involves the administration of the methylol-transfer agents taurolidine and/or taurultam. In one embodiment the taurolidine and/or taurultam compositions may be administered prophylactically to combat post-operative infection. Certain novel compositions comprising taurolidine and or taurultam are also described.
US20090062237 Evaluating immune competence This document relates to methods and materials involved in evaluating immune competence in a subject. For example, methods and materials for evaluating immune competence in a subject to BK virus (BKV) are provided. Also provided are isolated peptides, compositions, and methods useful for evaluating whether or not a subject is BKV immunocompetent. Also provided are methods for treating BK virus nephropathy in a subject that is BKV immune incompetent.
CN102617459A 1, 4-dihydroxy-2-formoxyl-9, 10 anthraquinone new acyl hydrazone compounds with antitumor activity and preparation method The invention discloses 1, 4-dihydroxy-2-formoxyl-9, 10 anthraquinone new acyl hydrazone compounds with antitumor activity and a preparation method. The concrete method comprises the steps as follows: 1, 4-dihydroxy-2-formoxyl-9,10 anthraquinone and a series of acylhydrazines can synthesize the 1, 4-dihydroxy-2-formoxyl-9, 10 anthraquinone new acyl hydrazone compounds; and better activity can be shown in the activity tests of cell cycle division protein 25B.
WO2006076284A3 AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE The present invention provides an amino-imidazolone compound of formula I Chemical formula should be inserted here as it appears on the abstract in paper form. Also provided are compositions and methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
WO2007042271A8 Nutraceutical composition for the treatment of muscle wasting The use of at least one component selected from the group consisting of EGCG, hydroxytyrosol, resveratrol and derivatives, metabolites or analogues thereof in the manufacture of a nutraceutical composition for the prevention and treatment of muscle wasting leading to muscle loss, atrophy and other associated muscle disorders in animals, in particular mammals including humans.
CN101897681A Method for preparing rifampicin oral preparation The invention discloses a method for preparing a new rifampicin oral preparation. The method comprises the following steps of: a, dissolving rifampicin serving as a raw material of which the amount is 1/4 to 1/6 that of chloroform with the chloroform, and adding polyethylene glycol, wherein the mass ratio of the polyethylene glycol to the rifampicin is 4-8:1; b, heating the mixture in water bath, and preparing solid dispersions after the chloroform finishes volatilizing; c, preparing the remaining rifampicin serving as the raw material into a soft material; d, pelletizing the soft material by using a 14 to 20-mesh screen, drying the particles, granulating the dried particles, adding an auxiliary material into the particles, and mixing the particles and the auxiliary material to obtain dry particles; and e, filling the solid dispersions and the dry particles into capsules or stamping the solid dispersions and the dry particles into tablets. The dissolution and quality stability of the rifampicin oral preparation are improved effectively.
CA2259707C Disinfecting and sterilizing concentrate containing an aromatic dialdehyde and a neutral ph buffering system A disinfecting and sterilizing concentrate containing an aromatic dialdehyde and a neutral pH buffering system is provided. Aromatic dialdehyde concentrations of greater than 5 w/w% are achieved while maintaining the stability of the buffering system. A method and a kit for preparing a disinfecting and sterilizing concentrate is also provided.
US20100216881 Enhydrazone esters for treating asthma, allergy and inflammation The enhydrazone esters for treating asthma, allergy, and inflammation relate to the use of two cyclohexenone derivatives and pharmaceutically acceptable salts thereof in the treatment of asthma, allergies, and inflammation. The esters have the formula: wherein R is ethyl or methyl. Administration of the esters inhibits the degranulation of eosinophils, the degranulation of mast cells, and the release or expression of tumor necrosis factor-α, thereby alleviating the debilitating symptoms of asthma, allergic reactions, and inflammatory responses.
WO2013071079A1 Lin28/let-7 crystal structures, purification protocols, and molecular probes suitable for screening assays and therapeutics The invention provides compositions and methods for regulating microRNA (miRNA) biogenesis. The invention also relates to compositions and methods for treating or preventing cancer in a subject in need thereof.
CN103285416A Chitosan antibacterial wound protection film The invention discloses a chitosan antibacterial wound protection film which consists of chitosan, glycerin distilled water and gelatin. The chitosan antibacterial wound protection film is simple in configuration, can promote solidification of blood, has the effects of realizing sterilization, promoting wound healing and absorbing wound exudates along with difficulty in dehydration and contraction.
US20120294801 Conjugates of rgd peptides and porphyrin or (bacterio)chlorophyll photosynthesizers and their uses Conjugates of porphyrin, chlorophyll and bacteriochlorophyll photosensitizers with RGD-containing peptides or RGD peptidomimetics are provided that are useful for photodynamic therapy (PDT), particularly vascular-targeted PDT (VTP), of tumors and nonneoplastic vascular diseases such as age-related macular degeneration, and for diagnosis of tumors by different techniques.
US20120142747 Compositions and methods for delivering clonidine to a target tissue site Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of immediate release clonidine and a sustained release clonidine at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days or longer.
US20110159087 Crosslinked Polymers Disclosed herein are pharmaceutical compositions comprising wet granulated bile acid sequestrants having the general Formula I shown, and their process of preparation. The present invention also discloses process for preparation of Colesevelam hydrochloride, an antilipemic agent.
WO2009002538A3 Amorphous erlotinib, processes for the preparation thereof, and processes to prepare additional forms of erlotinib The present invention provides amorphous erlotinib, processes for the preparation thereof, and processes to prepare additional forms of erlotinib (F).
US20080070887 Diaryl Ether Derivatives and Uses Thereof Compounds of Formula (I) that act as antagonists at the mu, kappa and/or delta opioid receptors and therefore useful in the treatment of diseases, conditions and/or disorders that benefit from such antagonism in animals are described herein. where R1, R2, R3, R4, R5, and R6 are described herein.
EP1392337B1 Pharmaceutical formulation consisting of a plant dry extract with a calcium coating The invention relates to a pharmaceutical formulation consisting of a calcium salt and of a plant dry extract and provided in the form of a coated tablet, whereby the formulation has a core comprised of at least one plant dry extract that is enclosed by at least one coating made of at least one calcium salt. The plant extracts used for the core can be selected among: Vitex agnus castus (chaste tree); Belamcanda chinensis (leopard flower); Cimicifuga racemosa (black cohosh); Trifolium pratense L. (red clover); Oenothera biennis hom. (evening primrose); Glycine soja (soybean); Serenoa repens (saw palmetto); Urtica dioica (stinging nettle), particularly the roots thereof; Cucurbita pepo (pumpkin), particularly the seeds thereof; Pygeum africanum; as well as suitable mixtures thereof.
US20110130464 Combination Agent for Improving Carcass Performance in Finishing Pigs A composition of ractopamine and astaxanthin, included as additives in a feed, for finishing hogs, improves carcass performance.
CN102670580A Preparation method for naftidrofuryl stereoisomer and medicine application The invention discloses a preparation method for naftidrofuryl stereoisomer and a medicine application, in particular to an application on preparing the medicines for treating peripheral blood vessel diseases, cardiovascular and cerebrovascular diseases and central nervous system diseases. The invention also relates to a method for preparing four stereoisomers of 2-(1-naphthyl methyl)-3-(tetrahydrofuran base) propionic acid. R-phenylethylamine and S-phenylethylamine are respectively used as resolving agents to respectively resolve 2-(1-naphthyl methyl)-3-(2'R-tetrahydrofuran base) propionic acid and 2-(1-naphthyl methyl)-3-(2'S-tetrahydrofuran base) propionic acid to correspondingly obtain four stereoisomers of the 2-(1-naphthyl methyl)-3-(tetrahydrofuran base) propionic acid. The preparation method related by the invention is convenient to operate and has a strong reproducibility, the resolving yield is improved to a certain degree, a small quantity of resolving agent is used, and the production cost is lowered.
US20080015182 Potent PARP Inhibitors The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), their preparation, and their use as inhibitors of the enzyme poly(ADP-ribose)polymerase for the preparation of drugs.
US7129358 Oxidizing the corresponding sulfide without sulfone production to product purer omerprazole, lansoprazole, pantoprazole, rabeprazole, etc. Improved processes for preparing substituted 2-(2-pyridylmethyl)sulfinyl-1H-benzimidazoles are disclosed.
US20080286338 Drug delivery system with scleral lens A scleral lens is provided with a drug that is retained in the reservoir of fluid between the scleral lens and the cornea. This system can be used to deliver drugs not currently used because of poor bioavailability, to increase bioavailability of drugs used in patients already wearing a scleral lens, and to improve bioavailability in patients who are not currently wearing the lens. Dosing can be provided less frequently, thus decreasing the risk of non-compliance.
WO2011154771A1 Use of 1-beta-d-ribofuranosyl-1h-1,2,4-triazole-3-carboxamide for the treatment of infectious salmon anaemia (isa) in salmonids The invention relates to the novel use of 1-beta-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide for the treatment of infectious salmon anaemia caused by the infectious salmon anaemia or ISA virus in salmonids
US20110165226 Influenza cap-leader sequence The invention comprises a viral cap-leader sequence which comprises at least three bases complementary to the 3′-ultimate residues of a (−)ssRNA virus template sequence. Preferably said consensus sequence is represented by the general formula 7mG(N)6-10-(A/U/G)−A/U−AGC, more preferably 7mG(N)7-8-(A/U/G)−A/U−AGC. Further comprised are modified cap-leader sequences that are able to block elongation by the viral polymerase or cleavage by the viral endonuclase. Such modified cap-leader sequences comprise a 3′-terminal phosphate group, one or more phosphorothioate or phosphorodiamidate bonds or one ore more morpholino rings. Also pharmaceutical products comprising such a modified cap-leader sequence are disclosed. Further, the invention comprises methods for inhibiting virus transcription, especially for influenza virus, using such a modified cap-leader sequence or pharmaceutical product.
EP1903028A1 Conjugates of glutamate and NMDA receptor channel blockers without excito-toxic effects Methods for delivering therapeutic amounts of glutamate to the CNS while simultaneously protecting against its excito-toxic effects are provided. By administering a blood-brain barrier-permeable Conjugate Compound, which comprises glutamate linked to an N-methyl-D-aspartate receptor antagonist, glutamate is released within the CNS for beneficial effect without causing excito-toxicity. Examples of such Conjugate Compounds are provided and their cognition-enhancing effect without engendering excito-toxicity in both normal and cognition-impaired animals is demonstrated.
WO2011083830A1 Novel anticancer agent and method for screening same Provided are: a method for screening a target protein for treating cancer, characterized by comprising culturing a mutant yeast, which carries a nucleic acid encoding a mammal-origin test protein, said nucleic acid having been transferred thereinto, and lacks of a cell cycle checkpoint factor, and a corresponding wild-type yeast, and selecting, as a candidate for the target protein for treating cancer, a protein inhibiting the growth of the mutant yeast but not inhibiting the growth of the wild-type yeast; a method for screening a substance having an anticancer effect, characterized by comprising culturing a mutant yeast, which carries a nucleic acid encoding the target protein for treating cancer obtained by the aforesaid method, said nucleic acid having been transferred thereinto, and lacks of a cell cycle checkpoint factor, in the presence of a test substance, and selecting, as a candidate for the substance having an anticancer effect, a test substance restoring the growth of said mutant yeast; a therapeutic and/or prophylactic agent for cancer which comprises a dynAP inhibitor having an Androstane skeleton, and so on.
EP2054381A2 Pharmacodynamic hybrids endowed of hypoglycemic and no-donor activities obtained combining hydroxylated derivatives of glibenclamide and nitrooxy-substituted carboxylic acids Compound featuring a hypoglycemic action and in the meantime a release of nitric oxide (NO), said compound having the following general formula (I) : where at least one among R, R1, and R2 is a substitute comprising an nitroxy-ester group bound to a acyl aliphatic, aromatic or aliphatic-aromatic group. The compound can be in particular, used to treat patients affected by NO endogenous deficit responsive to diabetes mellitus of type 2.
US20080138436 Food Supplement Composition Suitable For Promoting Iron Absorption Use of a composition comprising cartilage or chondroitin sulphate and absorbable zinc for the preparation of a food supplement or a drug suitable for promoting iron absorption in patients suffering from lack of iron.
EP2359818A1 Combination of LBH589 with HSP 90 inhibitors for treating cancer The invention relates to a combination comprising the N-hydroxy-3-[4-[[[2-(2-methyl-1 H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2E-2-propenamide; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.
US20080194534 Retinoic esters with cholesterol; antiproliferative agents; disorders caused by abnormal cellular differentiation; psoriasis, cancers of skin, colon, lungs, breasts, prostate, or ovaries, leukemia, neuroblastomas, eczema, acne; improved wrinkle resistance, skin hydration, sebum secretions A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group and the resulting modified retinoids are described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably a secondary or tertiary alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window. The modified retinoid compounds are useful in the treatment and prophylaxis of all diseases and disorders where retinoid compounds have been shown effective.
CN1823824A Medicine and food dual purpose nutritive product for preventing and treating synchysis and its manufacturing method A Western medicine used as both medicine and food for preventing and treating synchysis is prepared from vitamins and trace elements. Its preparing process is also disclosed.
US20120219626 Pharmaceutical Compositions of Sevelamer The invention relates to a pharmaceutical immediate release tablet comprising a core comprising 70-85 weight percent of sevelamer carbonate, calculated as an anhydrous compound, 10-25 weight percent of lactose monohydrate and, optionally, a water soluble film coat surrounding the to a process of making such tablets, to their use in medicine, and to the use of polyvinyl alcohol-polyethylene glycol graft copolymer for making such coated tablets.
CN102718703A Dimethyl-containing arylurea derivative with dual GK/PPAR agonist activities The invention discloses a novel arylurea derivative, its preparation method, a pharmaceutical composition and an application thereof. Specifically, the invention relates to an arylurea derivative as shown in the general formula I, its medicinal salt, a preparation method thereof, a composition containing one or more of the compounds, and an application of the compounds in treatment of glucokinase and peroxisome proliferator-activated receptor related diseases such as diabetes, obesity and the like.
CN101095693A Compound recipe medicine for treating dermatitis Disclosed is a pharmaceutical composition for treating skin diseases, wherein each 1g of the medicinal composition comprises doxepin 5-100mg, sodium heparin 20-400 IU.
US20100063146 Method for treating disorders related to complement activation A method for treating or preventing a complement activated T-cell mediated disorder in a subject includes administering a therapeutically effective amount of a pharmaceutical composition to the subject. The pharmaceutical composition includes at least one amidine compound or pharmaceutically acceptable salt.
WO2007080108A1 Composition ascorbic acid and a metal ion for selective killing of pathological mammalian cells The invention concerns a composition comprising vitamin C and/or derivates thereof and at least one metal ion for selective and efficient killing and/or destrcution of pathologically altered mammalian cells. The solutions according to the invention are applied intra-venously via blood or by direct injection into the pathologically altered united cell structure. Thereby these cells are efficiently and selectively killed and/or destroyed. Additional enhancement of this effect can be achieved by the optional application of substances that support up-take of metal ions into pathologically altered cells.
CN101284827B Antineoplastic compounds containing triazole ring naphthoyl imines and method for preparing same The invention provides an anti-tumor compound containing triazole cycle naphthalimide and a preparation method for the same, which belongs to the bio-organic synthesis field. The anti-tumor compound containing triazole cycle naphthalimide introduces five-member 1, 2, 3-triazole cycle on a naphthalimide matrix in a substituted group mode and designs, and synthesizes compounds through nitro reduction, diazotization, azide substitution reaction, Click Chemistry and amino condensation reaction. The compound has good anti-tumor activities, has better inhibition function on the normal growth of various tumor cells (such as human lung cancer, glial cancer and so on) from different tissues and hereditary variation cells( such as leukemia cell and so on) from different sources.
CN1919279A Plaster with wind and cold dispelling, toxin removing and clots absorbing function, and its preparing process The invention discloses a plaster for dispersing pathogenic wind and removing toxic substances from human body, which mainly comprises areca-nut, Chinese angelica root, Ligusticum wallichii, dahurian angelica root, ledebouriella root, Clematis chinensis, safflower, frankincense, panicled swallowwort root, campeachy wood, speranskia herb, buck grass, achyranthes and cyathula root, homalomena rhizoma, root of red rooted saliva, camphor, and sesame oil. The invention also discloses the process for preparing the plaster.
CN101669965A Application of PEG-PCL-PEG triblock copolymer in preparation of medical anti-adhesion material The invention relates to the field of medical high polymer materials, and in particular to an application of triblock copolymer in preparation of medical anti-adhesion material. The invention aims tosolve the technical problem of providing a new choice for medical anti-adhesion material, and has the technical scheme of providing the application of PEG-PCL-PEG triblock copolymer in preparation ofmedical anti-adhesion material, wherein the molecular weight of the PEG-PCL-PEG copolymer is from 1500 to 10000, the ratio of the molecular weight of the PEG chain to the molecular weight of the PCL chain is 0.4 to 2.6; and the triblock copolymer can be dissolved in water to form a solution and form gel after reaching a certain intensity. Experiments prove that water gel of the PEG-PCL-PEG triblock copolymer has many good characteristics, and provides a new choice for the field of medical anti-adhesion materials.
WO2012061708A1 Crystalline forms of hydrochloride salt of (4a-r,9a-s) -1- (1h - benzoimidazole- 5 -carbonyl) -2, 3, 4, 4a, 9, 9a - hexahydro -1h- indeno [2, 1 -b] pyridine- 6 -carbonitrile and their use as hsd 1 inhibitors The present invention relates to crystalline compounds of the following structural formula (II) possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
EP1087773B1 Vaginal active agent delivery procedures and formulations thereof Intra-vaginal delivery procedures including compositions and units therefor whereby an effective releasable amount of oestradiol 17β is released to achieve an efficacious effect insofar as oestrus expression is concerned. Preferably a cyclodextrin is utilised to enhance absorption.
CN101810639A Broad-spectrum touch-out medical bactericide and preparation method thereof The invention discloses a broad-spectrum touch-out medical bactericide and a preparation method thereof. The broad-spectrum touch-out medical bactericide comprises the following component in weight by percent: 5 to 15 percent of povidone iodine, 3 to 10 percent of medical Vaseline, 1 to 5 percent of nonoxynol nonylphenoxy-polyethoxyethanol and pure water. After the broad-spectrum touch-out medical bactericide is contacted with the surface of wound or the afflicted part, the iodine can be depolymerized and released to play the sterilization effect. The broad-spectrum touch-out medical bactericide has the advantages that: the thrill on the tissue is small, the bactericide is applicable to the skin and the mucous membrane infection, the pain and the damage caused by the thrill are greatly reduced compared with other ordinary medicine bactericide, and the bactericide can be directly used for the disinfection and abrasion. The broad-spectrum touch-out medical bactericide is of a broad-spectrum strong sterilization disinfectant and has strong killing effect on virus, bacteria, fungus and mycoticspore. The broad-spectrum touch-out medical bactericide has small thrill on the skin, low toxicity, duration and safe, simple and convenient application.
US20070299136 Crystalline and Amorphous Forms of Efaproxiral Sodium There are provided in accordance with the present invention crystalline forms A, B, C, F, G, I, J, P, and Q of efaproxiral sodium. Also provided is the amorphous form of efaproxiral sodium. Also provided are methods of forming the novel polymorphs and the amorphous form of efaproxiral sodium, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.
US7563765 Histidine-rich glycoprotein The invention relates to histidine-rich glycoprotein (HRGP) polypeptides and the use of these polypeptides. The invention includes methods for the inhibition of angiogenesis by administering an HRGP polypeptide. The invention also includes pharmaceutical compositions and articles of manufacture comprising HRGP polypeptides, antibodies and receptors that bind to an HRGP polypeptide, HRGP-depleted plasma and polynucleotides, vectors and host cells that encode HRGP polypeptides.
WO2012008697A3 Orally administered agent for increasing sperm count The present invention relates to an orally administered agent for increasing sperm count, and to an orally administered agent for improving sexual function, and more particularly, to an orally administered agent for increasing sperm count, and an orally administered agent for improving sexual function, which use Decursin and Decursinol angelate as active ingredients. Said ingredients have the effects of increasing sperm count and enlarging the size of the prostate, kidneys, epididymis, penis, etc. which induces the advancement of sexual function, prevents reduction in sperm count brought about by the environmental hormone Bisphenol A, and restores sperm count. The orally administered agent for increasing sperm count and the orally administered agent for improving sexual function according to the present invention have the effects of increasing sperm count and enlarging the size of the prostate, kidneys, epididymis and penis, and are useful inventions having industrial applicability.
WO2013119910A1 Combination of muscarinic receptor antagonists and beta- 3 adrenoceptor agonists for treating overactive bladder Pharmaceutical combinations comprising a beta-3 adrenergic receptor agonist and a muscarinic receptor antagonist, and methods for their use are disclosed. Methods of using the pharmaceutical combinations for the treatment of one or more symptoms associated with overactive bladder, for example, frequency of urgency, nocturia, and urinary incontinence, are also disclosed.
CN1771985A Application of chitin in preparing product for regulating body's acid-base equilibrium The present invention discloses the application of chitin in preparing produce for regulating bodyí»s acid-base equilibrium. The chitin has the functions of raising pH value of cell survival environment, reducing the damage of acid environment on cell, regulating the pH value of environment inside body and maintaining the normal metabolism of organism.
WO2012135597A3 Novel, protective, anti-inflammatory receptor and its use in preservation of mitochondrial function, wound healing and repair Provided herein is a novel mitochondrial Angiotensin II type 1 and type 2 AT1R and AT2R receptor which plays a role in protection of mitochondria against oxidative damage. Evidence from animal studies indicates a role for this receptor in preservation of mitochondria and up-regulation of survival genes, anti-inflammatory action, and improvement of wound healing in the skin and soft tissues. Pharmaceutical compositions for treatment directed to preserving mitochondrial function, anti-inflammation, wound healing and decreasing the signs of aging, as well as medicaments and their use are also provided.
US20070264331 Stable pharmaceutical composition of immediate-release glimepiride and extended-release metformin This invention is directed to a pharmaceutical composition in the form of a tablet with improved stability, as well as the process for obtaining said composition. The tablet of the present invention comprises two active ingredients comprising two oral hypoglycemic agents: one phase with a sulphonylurea, such as immediate release Glimepiride, and a second phase with a biguanide, such as extended-release Metformin hydrochloride (Metformin HCl). The biphasic tablet, which can include over 500 mg of Metformin HCl (i.e. up to 1,000 or 1,500 mg, depending on the daily requirements of each patient), is to be orally administered once or twice a day. The combination of these hypoglycemic agents has a synergic effect and therefore a greater effectiveness in controlling the blood glucose level in patients with diabetes mellitus, type 2.
CN1939312A Usage of copper complex A medical application of copper complex in relieving inflammation, analgesia, haemostasis, and treating toothache, dentin hypersensitiveness, oral ulcer, etc is disclosed. Said copper complex is prepared from copper green and acetylsalicylic acid through chemical reaction.
US20090076043 Deuterium-enriched alfuzosin The present application describes deuterium-enriched alfuzosin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2007080170A1 CRYSTALLINE FORM OF 1´-(1-METHYLETHYL)- 4´-[(2-FLUORO-4-METHOXYPHENYL)METHYL]-5´-METHYL-1H-PYRAZOL-3´-O-β-D-GLUCOPYRANOSIDE, A METHOD FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS The invention relates to a crystalline form of 1´-(1-methylethyl)- 4´-[(2-fluoro-4- methoxyphenyl)methyl]-5´-methyl-1H-pyrazol-3´-O-β-D-glucopyranoside, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
CN102258474B Preparation method of self-microemulsifying coenzyme Q10 powdery dry emulsion The invention relates to a preparation method of a self-microemulsifying coenzyme Q10 powdery dry emulsion. The self-microemulsifying coenzyme Q10 powdery dry emulsion is prepared from materials of, by weight: 1 to 40% of coenzyme Q10, 5 to 50% of an emulsifier, 1 to 30% of an auxiliary emulsifier, 10 to 70% of polysaccharide, and 0 to 1% of an anti-oxidant. The preparation method comprises stepsthat: (1) the emulsifier and the auxiliary emulsifier are heated until melted; (2) coenzyme Q10 is added to a liquid obtained in the step (1), and is dissolved by stirring, such that an emulsified crude oil is obtained; (3) 0.2 to 0.5 times of pure water is added to the emulsified crude oil obtained in the step (2), the mixture is processed through ultrasonic emulsification for 5 to 60 minutes, such that a W/O type emulsion is obtained; (4) under a condition of ultrasonic emulsification, pure water with an amount 10 to 100 times that of the pure water added in the step (3) is slowly added to the W/O type emulsion obtained in the step (3) within 30 to 240 minutes, such that an O/W type crude emulsion is obtained; (5) ultrasonic emulsification is stopped, polysaccharide is added to the O/W type crude emulsion obtained in the step (4), the mixture is stirred until no solid particle is left, such that a mixed emulsion is obtained; (6) high pressure homogenization and/or ultrahigh pressurehomogenization is carried out upon the mixed emulsion obtained in the step (5) at least one time, such that a microemulsion is obtained; (7) the microemulsion obtained in the step (6) is dried, such that a dry emulsion is obtained. The method provided by the invention is suitable for medical use.
US20110092459 Alpha helix mimetics and methods relating thereto Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
CN1623550A Hydroxy progesterone caproate oral preparation and its use An orally taken medicine of hyproval-PA in the form of tablet, capsule, soft capsule, instant particles, etc for treating breast cancer and functional metrorrhagia is disclosed. its advantages are high biologic utilization rate and high curative effect.
CN102973622A Bone-strengthening preparation formula for old people The invention discloses a bone-strengthening preparation formula for old people.The bone-strengthening preparation formula for old people has effects of improving human body microcirculation, renal functions and a human body histocyte oxygen-carrying level and can improve sclerotin conditions. The bone-strengthening preparation formula for old people comprises propolis, ginsenoside, calcium citrate and vitamin D3.
WO2005095364A1 Phenoxyacetic acid derivative and medicine containing the same A novel compound having excellent PPARα/Ϝ agonistic activity and having desirable properties required of medicines. It is a peroxisome proliferation-activated receptor α/Ϝ agonist represented by the following general formula (I) (wherein Q represents an optionally substituted benzene ring or pyridine ring; R1 and R2 each represents an optionally substituted, phenyl or 5- or 6-membered aromatic heterocyclic group; X, Y, and Z each independently represents carbon, oxygen, sulfur, or nitrogen; R3 to R9 each represents hydrogen, lower alkyl, etc.; and n is an integer of 0 to 3).
CN101805298A Novel aryl- and heteroarylpiperazines Novel aryl- and heteroarylpiperazines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
WO2009139085A1 Antitumor agent, kit, and method for treating cancer Disclosed are an antitumor agent comprising (1) a combination preparation of tegafur, gimeracil, and oteracil potassium, (2) at least one component selected from the group consisting of folinic acid and pharmaceutically acceptable salts thereof, and (3) cis-oxalate(1R,2R-diaminocyclohexane)platinum(II) in combination; a kit comprising a combination of a pharmaceutical composition for treating cancer in a mammal comprising (a) a combination preparation of tegafur, gimeracil, and oteracil potassium in an amount effective for treatment, (b) a composition containing at least one component selected from the group consisting of folinic acid and pharmaceutically acceptable salts thereof in an amount effective for potentiating an antitumor effect, and (c) a composition containing cis-oxalate(1R,2R-diaminocyclohexane)platinum(II) in an amount effective for potentiating an antitumor effect; and a method for treating cancer.
US20090163581 Pharmaceutical Products for Treating Neoplastic Disease and Inflammation Disclosed in certain embodiments is a pharmaceutical formulation and a functional food comprising a pharmaceutical ingredient comprising an active agent combination comprising flavonoids and tocotrienols in a ratio of about 75:25 to about 95:5 and at least one pharmaceutically acceptable excipient and methods to treat neoplastic diseases and inflammation.
CA2223608C Vaccine for porcine reproductive and respiratory syndrome virus The present invention provides a purified preparation containing, for example, a polynucleic acid encoding at least one polypeptide selected from the group consisting of proteins encoded by one or more open reading frames (ORF's) of an Iowa strain of porcine reproductive and respiratory syndrome virus (PRRSV), antigenic regions of such proteins which are at least 5 amino acids in length and which effectively protect a porcine host against a subsequent challenge with a PRRSV isolate, and combinations thereof in which amino acids non-essential for antigenicity may be conservatively substituted. The present invention also concerns a polypeptide encoded by such a polynucleic acid; a vaccine comprising an effective amount of such a polynucleic acid or protein; antibodies which specifically bind to such a polynucleic acid or protein; methods of producing the same; and methods of protecting a pig against a PRRSV, treating a pig infected by a PRRSV, and detecting a PRRSV using the same.
CN101361733A Use of flavone derivates and preparation method thereof The invention relates to the medicine field and provides an application of flavone derivative as anti-oxidation and anti-anoxia drugs or food. The compound has the structural formula on the right. The preparation method of the flavone derivative comprises the following operation steps: the whole herb of Uncinata Spikemoss Herb is ground and extracted by solvent or water in a reflux way; an initial extract is obtained by filtering or centrifugally removing undissolved substances and decompression drying; the initial extract is dispersed in water of equal volume and again extracted by chloroform, ethyl acetate and normal butanol sequentially; ethyl acetate extract liquor is taken and decompressed and dried in vacuum to obtain the ethyl acetate extract; and the flavone derivative is obtained by chromatography separation and refining.
CN102579412A External medicament for treating infant hemangioma and preparation method thereof The invention discloses an external medicament for treating infant hemangioma and a preparation method thereof, which belong to the technical field of medicine. The external medicament comprises the following components: propranolol, stearic acid, glycerin monostearate, white Vaseline, azone, oleic acid, Tween-80, glycerol, deionized water and ethylparaben. The method comprises the following steps of: accurately weighing a certain amount of greasy component and a certain amount of water-soluble component respectively, and heating and preserving heat respectively at 75+/-2 DEG C; and slowly adding the greasy component into the water-soluble component, and continuously stirring along the same direction till the mixture is fully emulsified and is condensed into paste. The external medicament is safe and reliable. As proved by clinical experiments, after the external medicament is uniformly smeared onto the surface of a tumor body, the tumor body is faded remarkably 2-3 months later, 59 percent of infant patients can be cured 5-7 months later, 33 percent of tumor bodies are faded remarkably, and the total yield is 92 percent.
CN102125574A Medicinal composition for suppressing tumors The invention discloses a medicinal composition for suppressing tumors. The medicinal composition for suppressing tumors comprises Rp1 and at least one of the following substances: C-K, Rh2 and Rg3, wherein the Rp1 has a structural formula I; the C-K has a structural formula II; the Rh2 has a structural formula III; and the Rg3 has a structural formula IV. The medicinal composition has a higher suppression effect on the growth of tumor cells. The formula I is shown in the specification.
CN101697994A Radiation-resistant and fatigue-resistant agent and preparation method thereof The invention discloses a radiation-resistant and fatigue-resistant agent and a preparation method thereof, relating to an agent and a preparation method thereof. The invention solves the problems that the existing radiation-resistant appliance only can be externally used while can not be internally used to actively resist the radiation and the existing radiation-resistant chemical medicine has high toxicity and bad effect. The agent consists of acanthopanax, astragalus mongholicus, herba epimedii and beta-carotene. The preparation method comprises the steps of: 1. weighing raw materials; 2. preparing acanthopanax extractive, astragalus mongholicus extractive and herba epimedii extractive; and 3. mixing the raw materials to obtain the agent. The agent is non-toxic, can actively resist the radiation form the internal to the external, and has good radiation-resistant and fatigue-resistant effect.
US20120165373 Method of Treating Skin with microRNA Modulators Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that suppress or down-regulate microRNA expression in dermal fibroblast, resulting in enhanced production of collagen, elastin and/or fibrillin in the skin. Also provided are methods for screening for activity against specific microRNAs and the methods of using active agents identified by the screening protocol in the treatment of skin.
CN102631348A Application of 4-alkyl-6-aryl-1, 3-thiazine in preparation of antidepressant drug The invention provides 4-alkyl-6-aryl-1, 3-thiazine shown in the chemical structural formula I and an application of the pharmaceutically acceptable salt of the 4-alkyl-6-aryl-1, 3-thiazine in preparation of an antidepressant drug, wherein R1 is selected from H, COCH3, COC2H5 or COC3H7-n; R2 is selected from H, C1-C2 alkyl, C3-C4 linear alkyl or branch alkyl; R3 is selected from H, COCH3 or CO2R (R is C1-C2 alkyl, C3-C4 linear alkyl or branch alkyl, or CH2CH2OCH3); X1, X2 and X4 are selected from H, methyl, ethyl, chlorine, bromine, fluorine, hydroxyl, methoxy group, ethyoxyl, nitryl, trifluoromethyl, chloromethyl or acetoxyl group; and X3 is selected from H, methyl, ethyl, chlorine, bromine, fluorine, hydroxyl, methoxy group, ethyoxyl, benzyloxy, nitryl, trifluoromethyl, chloromethyl or acetoxyl group.
EP1087781B1 Dietary supplement for supporting cerebrovascular tone The present invention relates to a dietary supplement for the support of normal cerebrovascular tone. Extracts of the feverfew plant in combination with magnesium and riboflavin, either singly or in combination provide the major therapeutic enhancement in the reduction of migraine headaches and the associated symptoms.
US20110071170 Tricyclic pyrazolopyrimidine derivatives A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1).
WO2005108355A2 Dihydrobenzothiophenes The invention relates to compounds of formula (I), in which W, R1, R2, R3, R4, and q are defined as cited in claim 1. One application for said compounds is the treatment of tumours.
WO2007047492A3 Increasing thymic output in hiv-negative patients with antiretrovirals A method of increasing thymic output in an HIV-negative patient, comprising the steps of (a) identifying a HIV-negative patient who is in need of increased thymic output and (b) supplying an effective amount of antiretroviral agent to the patient such that the patient has an increase in naÊve T-cells, particularly a patient suffering from idiopathic CD4 lymphocytopenia.
CN1858216A Gamma-linolenic acid dry microbial powder enriched with organic celenium and its producing process The present invention relates to dry gamma-linolenic acid thallus powder with rich organic selenium and its production process, as well as the mutagenesis strain for biosynthesis of the thallus powder. Under the action of the mutagenesis strain CGMCC N0.1652, and through selenium-enriching fermentation in culture medium with organic nitrogen source, inorganic salt and sodium selenite, gamma-linolenic acid thallus with rich organic selenium is obtained. Through further microwave vacuum and freeze drying, dry gamma-linolenic acid thallus powder with oil and fat content 35-39%, gamma-linolenic acid content 15-18% and selenium content 139-330 ppm is produced. The present invention has the features of simple production process, environment friendship, etc. and the produced dry gamma-linolenic acid thallus powder with rich organic selenium may be used widely in medicine, food, feed additive and other fields.
US20100261667 3-ß-D-RIBOFURANOSYLTHIAZOLO[4-5-d]PYRIMIDINE NUCLEOSIDES AND USES THEREOF The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyrimidine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.
CN102973743A Clear vision capsule The invention relates to a herbal compound capsule, and particularly to a herbal compound capsule for treating and preventing senile retinopathy and macular degeneration and a use method thereof. The capsule comprises the following main components by percentage: 30% of lutein, 8% of wolfberry fruit, 8% of grifola, 8% of cassia seed, 8% of ligustrum lucidum, 8% of buerger pipewort flower, 8% of rhizoma alismatis, 5% of astragaloside, 5% of ginsenoside, 5% of panax notoginseng saponins, 5% of cordycepin and 2% of carotene. The twelve medicines are ultra-finely grinded, and are evenly mixed to prepare the capsule. The capsule 1.5-2 g is swallowed by boiled water after each meal, and one granule of idebenone is synchronously swallowed; capsule 30 mg is continuously taken for three or four months. During the medication, cigarettes and wine are forbidden, spicy stimulating foods are forbidden, and patients cannot be angry. The capsule is taken by 30 neurodeatrophia and macular hole patients and 5 patients after retina and submacular operations; capsule1.5-2 g is taken orally at each time, and one granule30 mg of idebenone is synchronously taken; the medicines are taken for three times per day, and are continuously taken for three or four months; all patients obtain satisfactory effect, and subjective symptoms, such as blurred vision, dryness of two eyes, photophobia, tearing, swelling of eyes, and ophthalmalgia are obviously improved. And the naked vision is improved.
WO2011118759A1 Benzanilide derivative Provided is a novel COX-1 inhibitor. Specifically, disclosed are a benzanilide derivative represented by general formula (I), and a salt thereof. In the formula, R1 is selected from alkyl, alkenyl, hydrogen, benzyl, and phenethyl, R2 is selected from hydrogen, hydroxy, halogen, alkyl, alkoxy, and trifluoromethyl, and R3 is selected from hydrogen, acyl, and mesyl. W represents CH or N, and X-Y represents CO-NH or NH-CO.
WO2006100392A1 Novel use of tritoqualine for treating digestive inflammatory diseases and more particularly gastric and esophageal diseases The invention concerns the novel use of chemical substances, the levogyrous and dextrogyrous enantiomers of (AMINO-7 TRIETHOXY-4, 5, 6 OXO-1 DIHYDRO-1, 3 ISOBENZOFURANNYL-3) -1METHOXY-8 METHYL-2METHYLENEDIOXY-6, 7TETRAHYDRO-, 2, 3, 4ISOQUINOLINE or tritoqualine, in inflammatory pathologies relating to the digestive sphere and more particularly gastric diseases.
US7364919 Immobilization carbohydrates; calibration; diagnosis; antiinflammatory agents, bactericides Materials and methods for studying and modulating the interaction of carbohydrate-containing moieties with other species are described, in particular, small particles, e.g. clusters of metal or semiconductor atoms, which can be employed as a substrate for immobilizing a plurality of ligands comprising carbohydrate groups. These “nanoparticles” can then be used to study carbohydrate mediated interactions, e.g. with other carbohydrates or proteins, and as therapeutics and diagnostic reagents.
CA2749495A1 Novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives as gamma secretase modulators The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) wherein R1, R2, R3, R4, X, A1, A2, A3, A4, Y1, Y2, Y3 and Z have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
US20090306168 SirT Inhibitors That Bind to NAD Compound of formula (I) and methods of treating disorders by administering a compound of formula (I) are described herein. Examples of disorders include neoplastic disorders, fat-cell related disorders, neurodegenerative disorders, and metabolic disorders.
CN1796372A Antibacterial compound A-45, and application in preparing antibacterial drug This invention publishes an antibacterial compound A-45 with a common formula (I), its application in manufacturing antibacterial drugs and its blended composite drugs. This compound, with its pharmacologically permitted ester derivatives, ether derivatives, amino-formyl-N-alkyl derivatives and salts, performs outstanding and broad-spectrum antibacterial activity. It is especially germicidal to leptospiras and some other G- or G+ bacteria and is thus applicable in curing or preventing infection diseases.
US20050245577 Drug for kidney failure containing oxaluric acid derivative The effective ingredient of the agent for renal failure of the present invention is an oxaluric acid derivative having an excellent suppressive effect of the progression of renal failure. The oxaluric acid derivatives of the present invention have an excellent suppressive effect of the progression of renal failure to inhibit significantly the increase of creatinine level in blood accompanied by the progression of renal failure. The compounds of the present invention have highly safety with little side effects, so that they are very useful as an agent for renal failure which is required to be administered for long term.
US8710058 Polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof Compounds of the present invention concern 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The compound, 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile, has the following structural formula: The hydrochloride solvates and crystalline modifications thereof according to the invention are useful for treatment of physiological and/or pathophysiological conditions, such as cancer, that are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, especially Met-kinase. The present invention further relates to processes of manufacturing these crystalline modifications.
WO2012148929A2 Disorders implicating pufa oxidation Some aspects of the invention provide for a method of treating hepatic disorders, lipidemias and cardiac-related risk factors using polyunsaturated fatty acids which are modified in certain positions to attenuate oxidative damage by Reactive Oxygen Species (ROS) and/or suppress the rate of formation of reactive products and toxic compounds.
CN103385932A Navel-compressing drug for preventing and curing constipation after malignant tumor chemotherapy The invention discloses a navel-compressing drug for preventing and curing constipation after malignant tumor chemotherapy. The drug is composed of following raw materials in parts by weight: 10 to 30 parts of cistanche, 10 to 30 parts of rheum officinale, 6 to 20 parts of saltcake, 10 to 20 parts of fried semen raphani and 2 to 4 parts of borneol, then substrate, osmotic agent and lubricant are added into the raw materials to make a navel paste according to a ratio. The navel-compressing drug is used for curing constipation after malignant tumor chemotherapy and non-obstructive constipation caused by other reasons.
WO2008024026A3 Use of 9-oxoacridine-10-acetic acid, its salts and esters for the treatment, prophylaxis or relapse prevention of prostate cancer The present invention provides the use of 9-oxoacridine-10-acetic acid, its pharmaceutically acceptable salts and esters, in combination with antiandrogenic hormonotherapy, for the treatment, prophylaxis and relapse prevention of prostate cancer. A method of treatment or prophylaxis of prostate cancer comprises the steps of (a) administration of an effective amount of 9-oxoacridine-10-acetic acid, its pharmaceutically acceptable salt or ester to a patient in need thereof and (b) hormonotherapy aimed at decreasing androgen action. Further, a method of inducing or increasing the sensitivity of prostate cancer to hormone therapy aimed at decreasing androgen action is provided, wherein the method comprises administration of 9-oxoacridine-10-acetic acid, its pharmaceutically acceptable salt or ester.
US20060088542 Imidazoquinoline adjuvants for vaccines The invention relates to the fields of vaccines, vaccine adjuvants, molecular biology and immunology, and generally relates to adjuvants and nucleic acid immunization techniques. More specifically, the invention relates to certain adjuvant compositions, and to vaccine and/or nucleic acid immunization strategies employing such compositions.
CN103099815A Application of molybdenum in preparation of medicine for enhancing reproductive capacity of male rats The invention discloses application of molybdenum in preparation of medicine for enhancing reproductive capacity of male rats. The acceptable daily intake of molybdenum is 0.056-0.135mg. The certain amount of molybdenum can be effectively used for enhancing the reproductive capacity of male rats, has the obvious effect of enhancing the reproductive capacity of male rats and does not have an adverse effect.
WO2006071685A3 Antimicrobial combination therapy comprising an antibiotic and toxic compound selected from dna damaging agents, alkylating agents, heavy metal containing compounds and chelating agents This invention provides methods and pharmaceutical compositions for treating a subject having a condition associated with an antibiotic resistant bacterial infection. The invention includes administering to a subject a therapeutically effective combination of an antibiotic and a toxic compound (e.g., a nucleic acid damaging agent, an alkylating agent, or a heavy metal containing compound).
CN102440983A New medicinal application and pharmaceutical preparation of short-chain ceramide The invention relates to a new application of short-chain ceramide in preparation of anti-pancreatic-cancer medicines and a medically acceptable pharmaceutical preparation of the short-chain ceramide. The short-chain ceramide is matched with taxol to resist the pancreatic cancer, i.e. the short-chain ceramide is used as a sensitizing agent of the taxol. The short-chain ceramide and pharmaceutical preparation thereof can be combined with taxol to treat the pancreatic cancer, and have obviously better therapeutic effects for resisting cancers than gemcitabine.
WO2008095086A3 Topiramate plus naltrexone for the treatment of addictive disorders The present invention provides for the use of combinations of drugs to treat addictive disorders.
US6994959 which compete with DNA-binding sites of regulatory proteins which regulate t-cell activity (CD28 and cytokines), preventing transcription; analyzing immunocompetence; for treatment of autoimmune diseases Aptamer oligonucleotides specifically bind to the DNA binding site of proteins such as Sp1 and Sp1-related proteins which regulate the genes which encode costimulatory molecules such as CD28 and cytokines such as IL-2 and GMCSF. The oligonucleotides compete with the DNA-binding sites of regulatory proteins which specifically regulate molecules to modulate T-cell activation. This serves to modulate gene expression by preventing transcription of the gene. Aptamers are administered to provide therapies for diseases which involve aberrant T-cell activation such as psoriasis, Type I (insulin-dependent) diabetes mellitus, multiple sclerosis, autoimmune uveitis, rheumatoid arthritis, systemic lupus erythematosus, inflammatory bowel disease (Crohn's and ulcerative colitis), and septic shock and to regulate normal T-cell activation such as in allograft rejection.
WO2011040495A1 Heparanase-activity inhibitor, wrinkle ameliorating agent containing same, and pharmaceutical composition Disclosed is a heparanase-activity inhibitor containing as an active ingredient a 4-alkylresorcinol represented by the belowmentioned formula (I) (wherein R represents a straight-chain or branched alkyl group having 1-6 carbon atoms).
WO2006052976A3 Improved dosing regimen of temozolomide for treating cancer based on the patient’s mgmt level The use of temozolomide for the manufacture of a medicament for treating cancer in a patient in need of such treating is disclosed comprising administering temozolomide according to improved dosing regimen and/or schedules based on the patient's MGMT level. Additional improved dosing regimen and/or schedules for treating patients with temozolomide are also dislosed.
CN102512359A Mangiferin cream with anti-herpes simplex virus effect The invention discloses an external cream preparation for effectively treating herpes simplex virus (HSV) I type and II type infectious diseases and a preparation method as well as application thereof. The cream is prepared from high-purity mangiferin (purity of greater than or equal to 90 percent) serving as a raw material and proper auxiliary materials, wherein the mangiferin raw material is treated by using a micronization technique. Experiments prove that the cream has a good anti-herpes simplex virus effect, fast response and obviously shortened recovery time after the mangiferin raw material is micronized. The preparation method for the mangiferin cream is simple and convenient, and can be easily promoted to industrial large-scale production. Anti-herpes simplex virus pharmaceuticaleffect evaluation experiments and clinical pretests prove that the mangiferin cream has good curative effect on treatment of HSV-1 and HSV-2 infection, high safety and no toxic and side effects.
CN1857289A Dispersed compound tablet of glycyrrhizic acid and glycyrrhizinate and its preparing process The present invention discloses a kind of dispersed compound tablet of glycyrrhizic acid and its salt. The dispersed compound tablet consists of: glycyrrhizic acid or its salt or its lipoid ligand, amino acid, antioxidant stabilizer, disintegrating agent, filler, adhesive, lubricant, surfactant in certain weight proportion. The present invention also discloses the preparation process of the dispersed compound tablet. Compared with available tablet of glycyrrhizinate, the dispersed compound tablet has the advantages of fast acting, high bioavailability, less side effect, convenient taking, etc.
US20050084489 Synergistic administration of Vitaxin, a FAB fragment, or a competitive binding antibody for binding integrin alpha V beta 3 with the enzyme inhibitor; antiinflammatory, anticarcinogenic agents; autoimmune and metabolic bone disorders The present invention provides methods of preventing, treating, managing or ameliorating disorders utilizing an integrin αvβ3 antagonist in combination with an HMG-CoA reductase inhibitor and/or a bisphosphonate. The present invention also encompasses methods of preventing, treating, managing or ameliorating disorders utilizing an integrin αvβ3 antagonist in combination with an HMG-CoA reductase inhibitor and/or a bisphophonate, in further combination with another therapy (e.g., another prophylactic or therapeutic agent or treatment) which is not an integrin αvβ3 antagonist, an HMG-CoA reductase inhibitor, or a bisphosphonate. In particular, the present invention provides methods of preventing, treating, managing or ameliorating inflammatory diseases, autoimmune disorders, disorders associated with aberrant expression and/or activity of integrin αvβ3, disorders associated with abnormal bone metabolism, disorders associated with aberrant angiogenesis and cancers, or conditions associated therewith, utilizing an antibody that immunospecifically binds to integrin αvβ3 (e.g., VITAXIN®) in combination with an HMG-CoA reductase inhibitor and/or bisphosphonate, and optionally in combination with another therapy (e.g., another prophylactic or therapeutic agent or treatment) which is not an integrin αvβ3 antagonist, an HMG-CoA reductase inhibitor, or a bisphosphonate. The present also invention encompasses compositions and articles of manufacture for use in preventing, treating, managing or ameliorating inflammatory diseases, autoimmune disorders, disorders associated with aberrant expression and/or activity of integrin αvβ3, disorders associated with abnormal bone metabolism, disorders associated with aberrant angiogenesis and cancers, or conditions associated therewith.
WO2011031099A3 Ursodeoxycholic acid-synthetic hydrotalcite-eudragit hybrid, pharmaceutical composition containing the same and method for preparing the same The present invention relates to an ursodeoxycholic acid-synthetic hydrotalcite-Eudragit hybrid, a pharmaceutical composition containing the same and a method for preparing the same. The ursodeoxycholic acid-synthetic hydrotalcite-Eudragit hybrid according to the present invention is very useful as an active ingredient of a pharmaceutical composition because of its bitter-taste-blocking effect and improved body absorption rate with high solubility.
WO2010082503A1 Gold complex and medicinal composition containing same A novel gold complex which has potent antitumor activity and is effective when administered in a smaller amount, and a medicinal composition containing the complex. The gold complex includes, as a ligand, (R,R,R)-cis,cis-spiro[4,4]nonane-1,6-diamine, which is represented by stereostructural formula (A).
WO2013161929A1 Pyridinyl morpholinone derivative and drug composition containing same Disclosed is the compound represented in formula (I) or a pharmaceutically acceptable salt of same (in the formula: R1 is an aromatic carbon ring group or the like; -X- is a single bond, -O(C(R5a)(R5b))p- or the like; R5a and R5b are hydrogen atoms or the like; p is 0 or the like; R2 is a halogen or the like; n is 0 or the like; -Y- is a single bond, a substituted or unsubstituted alkylene or the like; R3 is a hydrogen atom or the like; R4 is a halogen or the like; and m is 0 or the like).
CN101366885A Centipede ointment for treating skin cancer The invention relates to a centipede paste for treating skin cancer. The centipede paste is characterized in that the preparation process of the centipede paste comprises the following steps of: extracting the concentrated solution of Chinese clematis, grassleaved sweetflag rhizome, asarum herb, Japanese dock root, boswellin, myrrh, pseudolarix, dandelion and the like to prepare an extract; mixing the extract with centipede powder, arenobufagin oil, borneol, camphor, realgar, lanolin and white Vaseline and stirring evenly into a semi-fluid; packaging the paste body through a packaging machine and obtaining the product after sterilization.
CN1823880A Preparation method of medicine or food for thinning reducing fat A medicine or health-care food for losing weight by inhibiting the sdsorption of choleaserol, promoting the degradation of choleaserol, decreasing the serum phosphatide, and speeding up the decomposing of fat is prepared from the refined extract of alfalfa, levo-carnitine, diluent, adhesive, flowing aid, and lubricant through proportional mixing, granulating, baking, and filling in capsules or tabletting.
WO2012018115A1 Composition for regeneratng normal tissue from fibrotic tissue The invention pertains to a pharmaceutical composition and method for regenerating normal tissue from fibrotic tissue that comprise a collagen-reducing substance. The invention makes possible the therapeutic regeneration of normal tissue from fibrotic tissue.
US20080311187 Crush resistan delayed-release dosage form The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substances (A) from the dosage form is at least partially delayed.
US20050113577 Such as hydrochloride salt 3-[5-(4-methanesulfonyl-piperazin-1-yl-methyl)-1H-indol-2-yl]-1H-quinolin-2-one; signal transduction; for treatment of angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, and inflammatory diseases The present invention relates to solid forms of the hydrochloride salt 3-[5-(4-methanesulfonyl-piperazin-1-yl-methyl)-1H-indol-2-yl]-1H-quinolin-2-one which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angio-genesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
WO2012120356A3 Process for the preparation of (s)-(+)-or (r)-(-)-10 hydroxy dihydrodibenz[b,f]azepines by enantioselective reduction of 10, 11-dihydro-10-oxo-5h-dibenz[b,f]azepines and polymorphs thereof The present invention provides a novel process for the preparation of substituted optically pure (S)-(+)- or (R)-(-)-10-hydroxy-dihydrodibenz[b, f]azepines or derivatives thereof, starting from 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepines using boronate esters or their derivatives. The- present invention also provides use of thus prepared (S)-(+)- or (R)-(-)-10-hydroxy-dihydrodibenz[b,f]azepines for the preparation of their ester such as (S)-(-)-10-acetoxy-10,11-dihydro-5H-dibenz[b, f]azepine-5-carboxamide or (R)-(+)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. The present invention also provides novel solid state crystalline forms J1, J2, J3, J4 and amorphous form of eslicarbazepine and the process for the preparation thereof. Also, the present invention provides novel solid state crystalline form and amorphous form of eslicarbazepine acetate and the process for the preparation thereof. The novel solid state forms of eslicarbazepine are useful for the preparation of derivatives of eslicarbazepine such as eslicarbazepine acetate.
WO2009136144A1 Purine derivatives suitable for the treatment of cancer, autoimmune and inflammatory diseases The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
US20060110333 Composition for nasal absorption This invention attempts to provide a composition for intranasal administration which has markedly lower risk of developing side effects compared to oral formulation, which promptly exhibits analgesic effects, and which has excellent bioavailability. The composition for nasal absorption comprises a carrier of calcium carbonate and/or calcium phosphate having an average particle size of 500 μm or less and an effective dose of an opioid analgesic uniformly distributed and attached to the carrier.
EP2301547A1 Use of activators of soluble guanylate cyclase for improving wound healing Use of six specific compounds (A), and their hydrates, salts and hydrated salts, to prepare a composition for promoting healing of wounds. Use of six specific compounds (A), of formulae (I)-(VI), and their hydrates, salts and hydrated salts, to prepare a composition for promoting healing of wounds. An independent claim is also included for a pharmaceutical composition for promotion of wound healing that contains (A). [Image] [Image] [Image] - ACTIVITY : Vulnerary; Antidiabetic. No biological data given. - MECHANISM OF ACTION : Guanylate cyclase activators.
CN101899043A Tylophora ovata base analogs with anti-tumor activity and preparation method and use thereof The invention discloses tylophora ovata base analogs with anti-tumor activity and a preparation method and a use thereof. The tylophora ovata base analogs can be applied in the preparation of drugs for treating malignant tumors, leukemia and cancers, and the compound structural formula is as follows: R1, R2, R3 or R4 can be CH3O, R1R2, R3R4 and OCH2O, and R1, R2, R3 and R4 can not be CH3O at the same time. The tylophora ovata base analogs have the characteristics of high efficiency, low toxicity and significant role of inhibiting tumor cells, and can be applied in anti-cancer new drugs; the tylophora ovata base analogs are synthesized by adopting the one kettle way, the process is not separated, and final products are separated; and PIDA is added for synthesis, the synthesis route is simple, the efficiency is high and the cost is low.
US20110268820 Use of selective estrogen receptor modulator for joint fusion and other repair or healing of connective tissue Methods for facilitating joint immobilization or fusion using selective estrogen receptor modulator (SERM) such as raloxifene are disclosed. The SERM may be administered systemically or locally. In conjunction with SERM, other therapeutic agents such as calcium, vitamin D, bone morphogenetic protein may be administered simultaneously. The method can similarly be applied to facilitate bone repair, bone healing, and connective tissue healing processes in a patient.
WO2012056465A1 A process for preparing curcumin encapsulated chitosan alginate sponge useful for wound healing A process for preparing curcumin encapsulated chitosan alginate sponge comprising the steps of: incorporating curcumin in a fluid phase of oleic acid; subjecting the mixture to a step of emulsification with chitosan solution by homogenization; emulsifying the resultant solution with alginate solution by homogenization; lyophilizing the final emulsion by freeze drying to produce curcumin loaded AC sponge.
CN101991550B Norcantharidin tablet and preparation method thereof The invention discloses a norcantharidin tablet which comprises the following components in part by weight: 1 part of norcantharidin and 5-20 parts of excipient, wherein the excipient comprises an auxiliary material-I and a lubricant, and the auxiliary material-I accounts for 90-99.9% of the total weight of the excipient. The preparation method comprises the following steps of: firstly, fully mixing microcrystalline cellulose with lactose, adding water, stirring into a thick paste, and freeze-drying to prepare the auxiliary material-I; mixing the raw material norcantharidin with the auxiliarymaterial-I; and adding the lubricant, mixing and directly compressing into the tablet. The norcantharidin tablet provided by the invention has good stability, and the provided method not only realizes the preparation of the norcantharidin tablet by using the direct tablet compressing method but also solves the problem of poor uniformity of content of prepared granular bulk pharmaceutical chemicals.
CN103462980A Application of spirooliganones B in preparation of medicine inhibiting tubercle bacillus The invention discloses the application of spirooliganones B in preparation of the medicine inhibiting the tubercle bacillus. The spirooliganones B has remarkable activity in inhibiting the tubercle bacillus and good application prospects, and belongs to a brand new matrix type. The spirooliganones B has the advantages of being high in inhibitory activity for the tubercle bacillus and prominent in substantive features, and makes remarkable progress in prevention and treatment of infection of the tubercle bacillus.
CN102018659A Intestine positioning preparation of glycyrrhetic acid, glycyrrhetinic acid and salts of glycyrrhetic acid and glycyrrhetinic acid, and preparation method and application thereof The invention discloses an intestine positioning preparation of glycyrrhetic acid, glycyrrhetinic acid and salts of glycyrrhetic acid and glycyrrhetinic acid, a preparation method thereof and application thereof. The key point is to wrap glycyrrhetic acid or glycyrrhetinic acid or diammonium glycyrrhizinate and salt compounds thereof in the intestine positioning preparation. The preparation method comprises the following steps of: spraying a liquid medicament onto empty pill cores in a fluidized bed to prepare medicament carrying pill cores, and then wrapping an isolation layer, an enzyme sensitive coating and a pH sensitive coating on the pill cores. The preparation is applied to the preparation of medicaments for treating inflammatory bowel diseases, hepatitis, rheumatoid arthritis, asthma, bronchitis and skin inflammation.
CN103690533A Method for improving light transmittance of compound amino acid injection A method for improving the light transmittance of a compound amino acid injection is provided, wherein the light transmittance of the compound amino acid injection is improved by replacing a step of detecting a reducing sugar of a sorbitol solution with a step of detecting the light transmittance of a preparation material, namely the sorbitol solution. The sorbitol solution whose light transmittance is more than 99% is selected. The change of the light transmittance of the sorbitol solution before and after sterilization is less than or equal to 0.1%. According to the method for improving the light transmittance of the compound amino acid injection, the light transmittance of the compound amino acid injection is improved by replacing a step of detecting the reducing sugar of the sorbitol solution with the step of detecting the light transmittance of the preparation material, namely the sorbitol solution, so that the technical bias that the detection of the reducing sugar is the main detection project is overcome, the problems of lowered light transmittance and unstable product quality are solved, and the product quality is improved.
CN1977889B Medicinal composition of astragalus, salvia miltrorrhiza and oxymatrine, and its preparing method The present invention discloses a new medicine composition for curing hepatic diseases and its preparation method. It is formed from (by weight portion) 400-10000 portions of astragalus root, 200-6000 portions of salvia root and 10-200 portions of kurarinone, and also can be made up by using 2-200 portions of astragalus total saponin or astragalus polysaccharide, 2-200 portions of salvia total phenolic acid and 10-200 portions of kurarinone. Said medicine composition can be made into various dosage forms of oral preparation, injection and others. Said medicine composition can be used for curing diseases of viral hepatitis, medicamentous liver lesion, fatty liver and alcoholic hepatitis, etc.
CN103520096A Process for producing terbutaline sulfate injection The invention relates to a terbutaline sulfate injection and a production process thereof. Every 1,000ml of the terbutaline sulfate injection comprises the following components: 0.15-0.4g of terbutaline sulfate, 0.1-0.35g of sodium pyrosulfite, 0.05-0.2g of ethylene diamine tetraacetic acid, 7.0-11g of sodium chloride, and the balance of injection water, wherein the pH value of the terbutaline sulfate injection is 3.2-4.8. The terbutaline sulfate injection has a good effect on improving lung function; the production process disclosed by the invention can guarantee that the produced terbutaline sulfate injection can meet related parameter requirements.
CN103202910A Externally applied medicine bag for acupuncture points The invention discloses an externally applied medicine bag for acupuncture points. The medicine bag is filled with halite, wherein the hot-nature externally applied medicine bag for acupuncture points is filled with the following medicines in parts by weight: 50-100 parts of folium artemisiae argyi, 20-30 parts of fennel, 10-15 parts of angelica sinensis, 5-10 parts of fructus evodiae and 2-5 parts of pepper as well as 550-650 parts of halite, the cold-nature externally applied medicine bag for acupuncture points is filled with the following medicines in parts by weight: 50-100 parts of folium artemisiae argyi, 100-150 parts of gypsum, 20-40 parts of mint, 5-10 parts of chrysanthemum and 0.5-1.5 parts of borneol as well as 400-500 parts of halite. The hot-nature externally applied medicine bag for acupuncture points has the functions of warming channels and expelling cold and activating merdians to stop pain and adjuvant effects on treatment of various pains such as stoma ache, gasteremphraxis, stomach duct and abdomen crymodynia and dysmenorrheal. The cold-nature externally applied medicine bag for acupuncture points has the functions of inhibiting swelling, easing pain, alleviating inflammation and eliminating fatigue and adjuvant effects on treatment of headache, fever, swelling and pain in throat, tootache, sunstroke, scald, muscle strain and sprain.
US7176195 Treatment of nocturnal enuresis, nocturia, polyuria resulting from central diabetes insipidus, urinary incontinence or bleeding disorders such a hemophilia Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9–11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents
CN101156854A Method for preparing camptothecin medicine slow releasing microcapsule The invention relates to a preparation method of camptothecin drug slow release microcapsule. Firstly, camptothecin drug microcrystal is positioned into deionized water for ultra sonic dispersion, secondly, the dispersed camptothecin drug microcrystal is positioned into polycation solution for adsorption, centrifugation and washing, third, the camptothecin drug microcrystal adsorbing the polycation is positioned into polyanion solution for adsorption, centrifugation and washing, then the step two and the step three are repeated, and thereby the drug microcapsule with core-shell structure is obtained. The microcapsule is very stable, can realize controlled release of the drug, can be produced to be micron-nanometer drug oral liquid or injection, and also can be produced to be drug capsule, and tablets, etc. The process of the invention is simple, the reaction condition is mild, the operation is easy, the reproducibility is good, the environment is protected, the invention provides substantial foundation and technical support for the application and the research of the camptothecin and other drugs having the characteristics of high curative effect, but large toxicity and poor water solubility, and has good application prospect.
US20080009477 Arylalkyl Ureas As Cb1 Antagonists CB1 antagonists are provided. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 receptor modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using ligands for receptor localization studies and various in vitro assays.
US20080299176 Drug delivery device comprising crosslinked polyurethane-siloxane-containing copolymers A drug delivery device for placement in the eye includes a drug core comprising a hydrophobic pharmaceutically active agent, and a holder that holds the drug core. The holder is made of a material impermeable to passage of the active agent and includes an opening for passage of the pharmaceutically agent therethrough to eye tissue. The device includes polyurethane-siloxane-containing copolymers crosslinked with hydrophilic monomers.
CA2795991A1 Dhea bioadhesive controlled release gel The DHEA bioadhesive controlled release gel includes DHEA mixed in a polymeric gel for the purpose of treating atrophic vaginitis, vaginal dryness, dyspareunia, itching, burning, irritation, increase in pH and decreased vaginal flora. The gel adheres to vaginal tissue and protects the DHEA from systemic absorption, which prevents leakage, loss of DHEA, and elevated levels of systemic DHEA. The gel is configured to slowly erode over time so as to deliver a predetermined dose of DHEA to vaginal tissue and thereby promote local intracellular conversion to estrogens, androgens and progesterone so that normal levels of fluid in the vagina is produced. The gel also acts as a moisturizer. An adjustable applicator may also be provided to insure proper placement and dose of the DHEA.
US20100290992 Nanoparticle nucleic acid binding compound conjugates forming i-motifs The present invention concerns the field of nanoparticle bioconjugates which form an i-motif or an i-motif related structure (compositions) without or with at least one further nucleic acid binding compound. The i-motif base pairs can be charged or non-charged. Their assembly can be controlled by the pH value or temperature. At least one of these nucleic acid binding compounds has to be attached at least to a nanoparticle. The methods provide compositions used for DNA driven programmable nanoparticle assemblies, electronic circuits, diagnostic detection tools, biosensors, memory storage devices, diagnostic devices for biomolecule sequencing and detection, drug delivery, application in tumour diagnostics and treatment, nanomachines, nanofabrication, nanocatalysis, nanoarrays, and nanoscaled enzyme reactors.
US7157443 High molecular weight intracellular adhesin antigen; induction immunology response A high molecular weight polysaccharide intracellular adhesin (SAE) antigen having the general structure of poly-1,6,β-2-amidoglucopyranoside, which is variable substituted with N-acetyl and O-succinyl substituents is described. Also, a method is given for isolating this antigen from Staphylococcus aureus. The SAE can be used in a vaccine, either alone, conjugated to an immunogenic protein, and/or with an immunogenic adjuvant.
US7279467 Benzothiazole-and benzoxazole-4, 7-dione derivatives and their use as dcd25 phosphatase inhibitors The invention concerns the use as cdc25 phosphatase inhibitors, in particular cdc25-C phosphatase, and CD45 phosphatase, of compounds of general formula (I), wherein: W represents O or S. In accordance with the invention, the compounds of general formula (I) can in particular be used for preparing a medicine for cancer treatment
EP2483257A2 2,3,4-benzothiadiazepine-2,2-dioxide derivatives The present invention relates to compounds 2,3,4-benzothiadiazepine-2,2-dioxide derivatives and enantiomers of the general Formula (I) wherein 'a' represents single or double bond, R1 and R2 represent, independently, hydrogen, halogen, cyano, alkyl, alkoxy, trifluoromethyl, or if 'a' represents single bond, R1 and R2 together form =N-S-N= group, R3 and R4 represent, independently, hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl, R5 and R6 represent, independently, hydrogen, halogen, cyano, alkyl, alkoxy, trifluoromethyl and/or enantiomers and/or pharmaceutically suitable acid addition salts thereof. The invention further relates to a process for their preparation, medicaments containing said compounds and the use thereof for the treatment of disorders of the central nervous system.
US7071203 Anticancer agents ; skins, prostate glands, lungs, breasts, leukemia, central nervous system, colon Described are pharmaceutically acceptable salts of a compound of formula (I) its tautomeric forms, its stereoisomers or its polymorphs, which is obtained by treating the compound of formula (I) with an acid selected from the group consisting of hydrohalo acid selected from the group consisting of hydrochloric acid or hydrobromic acid, acetic acid; sulfuric acid, nitric acid, phosphoric acid, boric acid, perchloric acid, tartaric acid, maleic acid, citric acid, methanesulfonic acid, benzoic acid, ascorbic acid, salicylic acid and benzene sulfonic acid wherein R1 represents substituted (C1–C6) alkyl wherein the substituent(s) is selected from mono (C1–C6) alkylamino or di (C1–C6) alkylamino; R2 represents hydroxy; R3, R4 and R5 represent hydrogen; and R6 represents hydrogen, or substituted (C1–C6) alkyl, wherein the substituent(s) is selected from halogen, hydroxy or (C1–C6) alkoxy and methods for using these compounds.
CN103372009A Application of Chukrasone B in preparation of medicines for preventing and treating liver damage The invention discloses an application of Chukrasone B in the preparation of medicines for preventing and treating liver damage. The pharmacological study on the Chukrasone B shows that the Chukrasone B has a protection effect on mice acute liver injury induced by D-galactosamine (D-GalN) and CC14. Therefore, the Chukrasone B can be used for the preparation of the medicines for preventing and treating liver damage or hepatitis. The application of the Chukrasone B in the medicines for preventing and treating liver damage is disclosed by the invention for the first time. As the skeleton type of the Chukrasone B belongs to a bran-new skeleton type and the Chukrasone B has an unexpected strong activity on liver damage treatment effect, the possibility that other compounds provide revelation does not exist. The Chukrasone B has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for treating liver damage.
CA2815749A1 Ibat inhibitors for the treatment of liver diseases The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.
US20090036443 6-cyclohexyl-5-phenyl-4H-thieno[3,2-b]pyrrole-2-carboxylic acid, used for inhibiting hepatitis C virus polymerase or prevention and treatment of hepatitis C viral infections The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
US20110060058 Inhibition of the Survival of Ovarian Cancer by Cyclohexenone Compounds from Antrodia Camphorata The present invention relates to a novel application of a compound. The compound 4-hydroxy-2,3-dimethoxy-6-methyl-5-(3,7,11-trimethyl-dodeca-2,6,10-trienyl)-cyclohex-2-enone of the invention is isolated and purified from the extracts of Antrodia camphorata, which can be applied for inhibiting the survival of ovarian cancer cells and be used as a pharmaceutical composition to inhibit the ovarian tumor growth.
WO2010124521A1 Derivatives of rhein, preparation methods and uses thereof Provided are derivatives of rhein having the structure of general formula (I), their preparation methods and uses in the preparation of medicaments for treating metabolic diseases.
US20110263694 Use of Xanthone Derivatives as a Medicament for Cancer The invention relates to xanthone derivatives of formula (IA) or (IB) and their use for manufacturing a medicament for cancer, and in particular for chemotherapeutic resistant cancer. More particularly, the invention relates to compounds and compositions comprising such xanthone derivatives for the prevention and/or treatment for chronic leukemia and, for example, for chronic lymphocytic leukemia (CLL) or B-lymphoma.
WO2012140666A3 Herbal extracts and compositions prepared therefrom The present invention provides processes for the preparation of extracts of Cassia auriculata (CA) and compositions comprising an extract of the same. The present invention also provides pharmaceutically active compounds isolated from Cassia auriculata which are useful for the treatment of disorders which include diseases arising because of insulin resistance such as Type 2 Diabetes, obesity, cardiovascular diseases and associated increase in homocysteine.
WO2008120690A1 Optically active organic acid-bridged binuclear platinum (ii) complexes Optically active organic acid-bridged binuclear platinum (II) complexes represented by the general formula (I) or (I'): (I) (I') (wherein R1 and R2 may be the same or different from each other and are each hydrogen or alkyl, or they are bonded to each other at their respective ends to form alkylene; R3 and R4 may be the same or different from each other and are each hydrogen or alkyl, or they are bonded to each other at their respective ends to form alkylene; A is a single bond or methylene; and X- is an anion). The complexes have excellent anticancer effects and are useful as drugs, particularly anticancer drugs.
US8710034 Method and composition for improving skin barrier function The invention relates to a method for improving skin lipid barrier function by applying to the skin a composition comprising effective amounts of a protease inhibitor and a cell differentiation enhancer. The composition is useful in promoting skin lipid barrier repair and maintaining the integrity of the lipid barrier. In this regard, the compositions can be used in the treatment and prevention of dry skin, and associated chrono/proto-aging conditions, in the treatment and prevention of irritation on the skin, in the treatment and prevention of UV-related damage to the skin, and in the enhancement of the retention of self-tanning.
US20080021102 Method for the Management of Incontinence A composition and a dosage form are disclosed comprising oxybutynin alone/or accompanied by another drug indicated for therapy. A method is disclosed for administering oxybutynin alone/or accompanied by a different drug or for administering oxybutynin and a different drug according to a therapeutic program for the management of incontinence alone, and for other therapy.
EP1744756A1 Use of meloxicam formulations in veterinary medicine The invention is directed to the use of a formulation containing meloxicam or a pharmacologically acceptable meloxicam salt of an organic or inorganic base, one or more vehicles and one or more suitable additives for preparing a veterinary medical composition for intramammary treatment of inflammatory diseases in mammals, particularly mastitis. The intramammary administration leads to an effective concentration in the target tissue, which is achieved very quickly.
CN1853637B Use of pentacyclic triterpene compound as glycogen phosphorylase inhibitor An application of the pentacyclo-triterpenoid used as the glycogen phosphorylase for preparing the medicines to treat diabetes, ischemic cardiovascular and cerebrovascular diseases, and tumor is disclosed.
EP2758067A1 Romidepsin and 5 - azacitidine for use in treating lymphoma Methods of treating, preventing or managing lymphomas are disclosed. The methods encompass the administration of an HDAC inhibitor romidepsin and a DNA demethylating agent 5-azacitidine, also known as VIDAZA®. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed
DE102006015733A1 Use of buprenorphine compounds to treat emotionally unstable personality disorder, alcohol dependence or multiple substance dependence Buprenorphine compounds (I) are used to treat emotionally unstable personality disorder, alcohol dependence or multiple substance dependence. Buprenorphine compounds of formula (I) or their salts, esters, ethers, tautomers or hydrates are used to treat emotionally unstable personality disorder, alcohol dependence or multiple substance dependence. [Structure I, page 10] X : O, NH, 1-6C alkylimino or S; R1>-R4>H, 1-12C alkyl, 2-12C alkenyl, 2-12C alkynyl or (CH2)nR, all optionally substituted with halo, OH, NO2, NH2, mono- or di(1-6C alkyl)amino, guanidino or 1-6C alkoxy and optionally with a CH2 group replaced by CO; R : 3-8C (hetero)cycloalkyl, 3-8C (hetero)cycloalkenyl or 6-14C (hetero)aryl; n : 0-6. An independent claim is also included for a composition comprising a compound (I) and a kappa opioid receptor antagonist. - ACTIVITY : Tranquilizer; Antialcoholic; Antiaddictive. No biological data given. - MECHANISM OF ACTION : None given.
CN103083529A External medicament for treating trachitis The invention relates to an external medicament for treating trachitis. The external medicament is prepared by refining the following Chinese drugs: houttuynia cordata, lily, apricot kernel, tendril-leaved fritillary bulb, schisandra chinensis, Chinese rhubarb and borneol, wherein the external medicament is regulated with silkie egg white, is applied to Yongquan acupoints at two sides of a patient for 15 hours with an interval between 3 and 5 hours. The external medicament is applied continuously for 3 to 5 times, can be used for treating trachitis, emphysema and core pulmonale with a total effective rate of over 95 percent and a high cure rate, is an optimal external medicament for treating trachitis, emphysema and core pulmonale without any toxic or side effect, and is convenient to save, carry and use.
WO2011106168A1 Purine compounds for treating autoimmune and demyelinating diseases A compound of Formula (I), or a pharmaceutically acceptable salt thereof. Values and preferred values of variables A1, A2 and R1 are provided herein.
CN101559100A Acesodyne capsule for heart and stomach The invention discloses an acesodyne capsule for heart and stomach, which is prepared by Cinnamomum migao H.W.Li, borneol and auxiliary materials, wherein the auxiliary material is aluminium hydroxide. Compared with the prior art, the invention improves the compounding of the acesodyne capsule for heart and stomach, changes the existing auxiliary material starch into the aluminium hydroxide; the naphtha rich in the Cinnamomum migao H.W.Li is dispersed in the aluminium hydroxide in the form of micro-grains; the mixed medicated powder is not bonded again, can be crushed, sieved and filled with capsule conveniently, is extremely suitable for practical industrial production and is convenient for the medicine production enterprises to execute the GMP standard strictly. Simultaneously, the medical function of the aluminium hydroxide also improves the curative effect of the acesodyne capsule for heart and stomach.
US7795302 use of topical formulation for treating rosacea containing a combination of an antimicrobial and at least one of non-retinoid inhibitor of one of nuclear factor-k-beta, AP-1 protein, matrix metalloproteinases, CD14 Rosacea is treated with a composition comprising an antimicrobial and at least one of an anti-inflammatory and a non-retinoid inhibitor of at least one of NF-KB, AP-1, MMPs, adhesion molecules, TLRs, and CD14. The composition may further comprise a retinoid.
WO2014160873A1 Benzimidazolone derivatives as bromodomain inhibitors This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, and X are described herein.
US7217710 Pyrazolo-pyrimidine compound; anticancer agents Pyrazolo-pyrimidine derivatives are described herein. The described invention also includes methods of making such derivatives as well as methods of using the same in the treatment of diseases.
US20120035108 Spray base material including low-molecular gelator There is provided a spray base material that can be safely used with a sense of security, that prevents leakage of liquid from a spray container, that is sprayable under any condition (when inverted, for example), that is sprayable to achieve uniform coating of the surface of an object (surface to be sprayed) without scattering, that causes no dripping from a sprayed surface, and that is safe when sprayed on a skin surface and the like; and a spray base material with an excellent sprayability that can include both hydrophilic and hydrophobic low-molecular compounds such as physiologically active compounds and perfume components to be used in pharmaceuticals, agrochemicals, and cosmetics, and that has a sustained release property. A spray base material comprising an aqueous medium that is gelled by a low-molecular gelator in the medium, wherein the low-molecular gelator includes one, two, or more compounds selected from a group consisting of low-molecular compounds capable of gelling the aqueous medium via self-assembly.
CN103373969A Phenyl imidazole ring-substituted amide compounds as well as preparation method and application for same The invention discloses phenyl imidazole ring-substituted amide compounds having structure general formulas shown in formulas (I), (II) and (III) as well as a preparation method and an application for the same, and in particular phenyl tetrazole acetamide (N-alkyl) (thio) urea compounds, phenyl tetrazole acetamide (N-alkyl) amide compounds, phenyl triazole formamide N-alkyl (thio) urea compounds as well as a preparation method and an application for the same. Experimental results indicate that the compounds are capable of effectively inhibiting the proliferation of human liver cancer cells and human lung cancer cells, and low in toxicity on normal cells, as well as are recommended to be used for preparing anti-tumour medicines for treating liver cancer or lung cancer.
WO2006122409A1 Antimicrobial molecules and their uses The present invention relates with the identification and use of antimicrobial oligonucleotides that act by a sequence independent mechanism, and includes the discovery that the antimicrobial activity is greater for larger oligonucleotides.
EP2130831A1 CDC25 inhibitors The invention relates to pyridoquinolones, their synthesis and pharmaceutical use. The pyridoquinolones are useful as CDC25 inhibitors.
CA2271249C Macromolecular neuraminidase-binding compounds The invention provides novel macromolecules, methods for their preparation, pharmaceutical formulations thereof and their use as anti-influenza agents. The invention also provides a novel diagnostic method which can be used for detection of all types of influenza A and B virus. The macromolecular compound of the invention has attached to it one or more molecules (neuraminidase binders) which bind to the active site of influenza virus neuraminidase but which are not cleaved by the neuraminidase.
WO2005026159A1 Benzoxazole acetonitriles The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycernia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylarnino moiety.R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, CiC6-alkYl, C2-C6-alkenYl, C2-C6-alkynyl or Cl-C6-alkoxy, aryl, halogen, carboxy,aminocarbonyl, cyano or hydroxy.
US20060183692 Use of low molecular weight thrombin inhibitors in cholesterol-lowering therapy According to the invention there is provided a cholesterol lowering therapy method and a method for modification of lipid (triglyceride), lipoprotein, and apolipoprotein profiles associated with an increased risk of cardiovascular complications comprising the administration of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, to a patient in need thereof.
CN1850849A 25-hydroxy dioscin ketone, and its preparing method and use The invention discloses a 25-hydroxide radical canaigre soap alkone and the manufacture method and the application. It uses canaigre ssapogenin as raw material to take hydroxylating through streptomycete at 25 tertiary carbon site to gain 25-hydroxide radical canaigre soap alkone. It could be used to make new compound and drug to anti malaria and restrict the growth of tumor.
EP1385497B1 Prevention or treatment of breast, prostate and/or cervical cancer with n,n-dimethylglycine The invention relates to a method of treating, inhibiting the metastasis of, or preventing cervical, breast or prostate cancer comprising administering to a patient an effective amount of N,N-dimethylglycine or a pharmaceutically acceptable salt thereof.
WO2011153383A1 Methods of treating platinum-resistant recurrent ovarian cancer with 4-iodo-3-nitrobenzamide in combination with an anti-metabolite and a platinum compound The present invention provides a method of treating platinum-resistant recurrent ovarian cancer in a patient, comprising administering to the patient an effective amount of 4- iodo-3-nitrobenzamide or a metabolite or a pharmaceutically acceptable salt thereof; gemcitabine; and carboplatin.
US20110015198 Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism [Problem] To provide a melanin-concentrating hormone receptor antagonist useful as a pharmaceutical agent for central diseases, circulatory diseases, and metabolic diseases. [Means for Resolution] Provided is a diarylmethylamide derivative represented by formula (I): Wherein R1a, R1b, R2a, R2b, R3a, and R3b independently represent a hydrogen atom or the like, R4 represents a hydrogen atom, C1-6 alkyl, or the like, R5 represents a hydrogen atom or the like, Z represents C1-6 alkyl or the like, or R4 and Z together form a 4- to 6-membered nitrogen-containing hetero ring, Y1 represents H or the like, Y2 represents H, or Y1 and Y2 together form —O—CH2—, W represents C, SO, or the like, Ar1 represents 6-membered aryl or the like, Ar2 represents 6-membered aryl or the like, and ring A represents a benzene ring, a pyridine ring, or the like.
WO2007142349A1 Hair growth composition Disclosed is a hair growth agent having a novel mechanism of action. Also disclosed is a hair growth composition comprising the hair growth agent. More specifically, disclosed is a novel hair growth composition comprising at least one member selected from an epsilon-N-(gamma-glutamyl)lysine and a salt thereof.
WO2012019254A1 Derivatives of 6, 7-dihydro-3h-oxazolo [3, 4-a] pyrazine-5, 8- dione The present invention describes a series of derivatives of 6, 7-dihydro-3H-oxazolo [3, 4-a] pyrazine-5, 8-dione, mixtures thereof, their pharmaceutically acceptable salts, which are inhibitors of PDE-5, possessing vasodilatator properties and relaxing effects. In particular, the derivative (J¾)-3-(l,3- benzodioxol-5-yl ) -1- ( lH-indol-3-yl ) -7-methyl-6, 7- dihydro [1, 3] oxazolo [3, 4-a] pyrazine-5, 8-dione, its enantiomer (S) -3- (1, 3-benzodioxol-5-yl) -1- ( lH-indol-3-yl ) -7-methyl-6, 7- dihydro [1,3] oxazolo [3, 4-a] pyrazine-5, 8-dione. The present invention describes, additionally, processes for the preparation of said compounds, pharmaceutical compositions containing them, as well as uses as inhibitors of the enzyme phosphodiesterase type 5 (PDE-5) in the treatment of the erectile dysfunction and PDE-5 inhibitor treatable disorders.
US7601754 7-Ethyl-3-hydoxy-2-(3,4,5-trihydoxy-phenyl)-chromen-4-one, for example; exhibits anti-oxidative properties in biological systems; utility in a sunscreen or skincare composition or to treat conditions involving oxidative damage, especially curative or prophylactic treatment of Alzheimer's disease Novel flavonoid compounds having anti-oxidant activity are described. Formula 1. The compounds have been shown to exhibit anti-oxidative properties in biological systems and their utility in a sunscreen or skincare composition or to treat conditions involving oxidative damage, especially curative or prophylactic treatment of Alzheimer's disease or ischaemia-reperfusion injury, is described.
US20140121284 Stable Pharmaceutical Composition Provided is a stable pharmaceutical composition having as an active ingredient a therapeutically effective amount of R(+)-N-propargyl-1-aminoindan or a pharmaceutically acceptable salt thereof, an absorption modulator, and a diluent, wherein the absorption modulator is glycerin, and the diluent is anhydrous dibasic calcium phosphate (CaHPO4) or microcrystalline cellulose. The stable pharmaceutical composition in accordance with the present invention provides extremely low amount of R(+)-N-propargyl-1-aminoindan and could significantly reduce cost. Moreover, the anhydrous dibasic calcium phosphate (CaHPO4) used as the diluent could enhance fluidity and improve ingredients uniformity in powder molding process. The glycerin used as the absorption modulator could increase the absorption of active ingredient such as R(+)-N-propargyl-1-aminoindan.
CN101550145B Cefradine compound preparation method The invention provides a cefradine compound and a capsule preparation method thereof. The preparation method of the cefradine compound includes the following steps: cefradine is added into an acid solution and dissolves fully in ice water bath; active carbon is added for discoloration and the mixed solution is filtered and the filtrate is combined and then put into a container; the filtrate is stirred at the initial temperature of crystallization to constant temperature; alkaline liquor is gradually added; the magma is filtered after the temperature of the magma reduces to the crystallizationend temperature, washed with alcohol and dried in vacuum to obtain the compound. Based on the total weight of capsule, cefradine capsule comprises 20-70wt of cefradine, 0-60wt of filling agent, 0-10wtof disintegrating agent, 1-10wt of adhesive and 0.5-3wt of lubricant.
WO2007130860A2 Constrained compounds as cgrp-receptor antagonists The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
US20070105856 6-benzyl-3-(4-chlorophenyl)-2-(2,4-dichlorophenyl)-2,6-dihydropyrazolo[3,4-c]pyridin-7-one; eating and psychological disorders; obesity, alcoholism Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
WO2011150855A1 Micro-rna biomarkers and methods for diagnosis of early colorectal carcinoma and high-grade adenoma The invention provides diagnostic kits for identifying one or more mammalian target cells exhibiting early colorectal carcinoma or high-grade adenoma. The kits comprise a plurality of nucleic acid molecules encoding microRNA sequences, wherein the nucleic acid molecules are differentially expressed in target cells and control cells, and the nucleic acid molecules together represent a nucleic acid expression biomarker that is indicative for the presence of early colorectal carcinoma or high-grade adenoma. The invention further provides methods for identifying one or more mammalian target cells exhibiting early colorectal carcinoma or high-grade adenoma by using the nucleic acid molecules. Methods and pharmaceutical compositions for preventing or treating early colorectal carcinoma or high-grade adenoma are also disclosed.
CN101011456A Externally used antiphlogistic anti-allergic medicament stilbene pine cream for skin side effect of cortical hormone The invention relates to a method for using glucocorticoids and astragalus root/astragalus root extractive as astragalus root polysaccharide or astragalus root glycosides to prepare the drug with fewer side effects. The glucocorticoids can be used to treat dermatopathy, with serious side effect in large agent. The invention can improve the antiphlogistic function of glucocorticoids and reduce the side effect.
EP1781632A1 Pyrans for use in the treatment of infection There is provided a novel compound of the general formula (I), in which each R is hydrogen, aryl, C1-6 alkyl, trialkylsilyl, or acyl, each R1 is selected from hydroxy, C1-6 alkoxy and acyloxy; each R2 is H, C1-4 alkyl, trialkylsilyl or acyl; R3 is H or Me; and n is 0 to 5 any of the alkyl groups including alkyl groups in alkoxy, acyl and acyloxy groups which may be substituted by aryl, C1-4 alkyl, C1-4 alkoxy, hydroxyl, trialkylsiloxy or acyloxy groups. The compound is an analogue of epigalcatechin galate or epicatechin galate, with an amide bonding placed of the natural ester bond, with resistance to hydrolysis by esterase enzymes. The compounds may be used to modulate the resistance to β-lactam antibiotics of various infections, especially methicillin resistant staphylococcus aureus (MRSA). Pharmaceutical compositions containing the novel compounds and combinations of the novel compounds and β-lactam antibiotics are described.
CN103099816A Drug composition inducing mitochondrial apoptosis of multiple myeloma cells The invention provides a drug composition inducing mitochondrial apoptosis of multiple myeloma cells, wherein the drug composition is composed of 0.25-1Mum of As2O3 and 10-20Mum of cryptotanshinone. Experiments proof that arsenic trioxide and cryptotanshinone are combined to obviously induce apoptosis of a myeloma cell U266; and the action mechanism comprises that expression of inhibitors of apoptosis protein such as Bcl-2, surviving and XIAP is regulated down, pro-apoptotic proteins Bax and Bak are transferred, positioned and increased from cytoplasm to chondriosome, cytochrome C is released and increased from the chondriosome to cytoplasm, chondriosome apoptosis pathway labelled proteins Caspase9, Caspase3 and PARP (poly-ADP-ribose polymerase) are activated, and further the mitochondrial apoptosis of the myeloma cell U266 is induced. According to the drug composition, mitochondrial apoptosis is promoted to achieve the aim of inhibiting the multiple myeloma cells, so that an As2O3 and cryptotanshinone composition has a wide application and development prospect in preparation of a drug for inducing the mitochondrial apotosis of the myeloma cells.
CN101342366A SOD oxidation resistant composition and preparation thereof The present invention relates to a SOD antioxidant combination and a preparation method thereof. The combination contains uperoxide dismutase preparation, propolis powder, vitamine E, vitamine C and spirulina platensis geitler; wherein, in the combination, the weight proportion of propolis powder, vitamine E, vitamine C and spirulina platensis geitler is as follows: 35 to 55 : 2 to 5 : 15 to 25 : 25 to 30; each 100g of the combination contains 40000 to 4000000 activity units of uperoxide dismutase. The uperoxide dismutase preparation is first uniformly mixed with part of the vitamine E; then the rest of the vitamine E is added into the multi-stage mixture and mixed to produce a binary mixture; the spirulina platensis geitler which is weighed according to the weight proportion is added into the binary mixture and uniformly mixed; then the propolis powder which is weighed according to the weight proportion is added into the binary mixture and uniformly mixed; finally, the vitamine C which is weighed according to the weight proportion is added into the binary mixture and uniformly mixed, and the antioxidant combination is produced. The antioxidant combination, which has an antioxidation function, can alleviate physical fatigue and enhance the immunity of the human body.
WO2006100710A1 Preventive or therapeutic composition for severe acute respiratory syndrome A preventive or therapeutic composition for severe acute respiratory syndrome that acts promptly with high safety. There is provided a preventive or therapeutic composition for severe acute respiratory syndrome, comprising catechins, characterized in that epigallocatechin gallate is contained in the composition in a weight ratio of 0.3 to 0.8 based on the total weight of catechins.
CN103356860A Amla weight-losing capsule The invention relates to an amla weight-losing capsule and belongs to the field of pure vegetal capsule medicine products. The amla weight-losing capsule comprises the following components: an amla extractive, an aloe extractive, marine polysaccharide, a bitter gourd extracting solution, radix puerariae and lotus leaf powder. The amla weight-losing capsule disclosed by the invention takes the amla as a main component, has multiple excellent effects of keeping body cholesterol content, reducing fat, losing weight, resisting cancer, preventing aging, promoting cell metabolism, supplementing nutrients needed by skin growth, and the like. The amla weight-losing capsule puts the pharmacodynamic effects into full play, is favorable for elimination of excess fat and proud flesh in a body, is capable of promoting the metabolism of a human body and delaying senescence.
CN101245091A Novel antineoplastic compound Ananaside B in thelenota ananas The invention relates to the field of medical technology, in particular to an anti-cancer compound Ananaside B which is separated from thelenota ananas, and the molecular formula is C54H87O26SNa. The chemical structure and the spatial configuration of the compound are determined by various modern spectral analysises, in particular to the comprehensive analysis by applying the advanced two-dimensional nuclear magnetic resonance spectra and high resolution mass spectra. In vitro anti-tumor trials show that the compound has significant inhibition function on A-549 lung cancer and IA-9 ovarian cancer and other 10 kinds of tumor cell strains. The compound can provide a lead compound for the development of new anti-tumor drugs, which has important values for the development and the utilization of the marine medicinal and biological resources of China.
WO2011037411A3 Composition comprising s-allyl-l-cysteine as active ingredient for preventing or treating gastrointestinal disorders A composition including S-allyl-L-cysteine as an active ingredient and having an anti-Helicobacter pylori activity or a gastric mucosa protective effect, a composition for preventing, relieving, or treating gastrointestinal disorders, and a method of using the compositions.
EP2107907B1 Combination of pemirolast and ramatroban for use in the treatment of inflammatory disorders There is provided combination products comprising (a) pemirolast, or a pharmaceutically-acceptable salt or solvate thereof; and (b) ramatroban, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in the treatment of atherosclerosis and related conditions.
CN102949564A Preparation method of Yinbing acne-elimination tincture The invention relates to a preparation method of a Yinbing acne-elimination tincture and belongs to the field of drug production processing. The Yinbing acne-elimination tincture has functions of treating various whelks and acnes, calming nerves, diminishing inflammation and relieving itching. The preparation method comprises the following steps of raw material preparation, proportioning, extraction, preparation, loading and outer packaging.
CN102839206A Preparation method for promoting self generation of human bone marrow hematopoietic stem cells The invention provides a preparation method for promoting generation of human bone marrow hematopoietic stem cells, and relates to a manufacture method of stem cells preparation. The method successively comprises the following steps of: a, collecting bovine placenta and fetal bovine marrow; b, cleaning, and sterilizing; c, separating protein, fat and active materials through a freezing centrifugal machine in an ultrafiltration method, so that the sediment is obtained; d, adding pepsase; e, adding water, and extracting to obtain fetal bovine marrow active polypeptide; f, getting the fetal bovine marrow active polypeptide, banana seedcase element and echinacea polysaccharide to be uniformly mixed to obtain marrow polysaccharide; g, getting the marrow polysaccharide, adding the water, and adding strontium, zinc, selenium, iodine, metasilicic acid, calcium, magnesium, potassium, sodium, iron, copper, lithium and nickel, and adjusting a pH value to be alkalescent, and then compounding to obtain a biological activity oral liquid preparation suitable for a human body. The preparation method has the beneficial effect that the human medullary hematopoiesis can be promoted to produce the hematopoietic stem cells; and an unique effect of treating various diseases can be achieved; and the preparation method is safe, efficient and has low cost, and prevention, health care and treatment effects can be achieved.
US7582651 Pyrrolopyridine derivative and use thereof A novel pyrrolopyridine derivative which is a compound represented by the formula wherein Ring A represents an optionally substituted pyridine ring; X represents an electron-attracting group; Y represents an optionally substituted divalent C1-6 chain hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; and R2 and R3 each independently represents hydrogen, an optionally substituted hydrocarbon group or an optionally-substituted heterocyclic group, or R2 and R3 may form an optionally substituted ring in cooperation with the adjacent nitrogen atom, or a salt of the compound. The pyrrolopyridine derivative has vanilloid receptor agonist activity and is useful as medicines such as a preventive/therapeutic agent and analgesic for overactive bladder.
US20080317835 Personalized Nutrient Deficiency Assay Methods Assays are preformed to determine nutrient deficiency levels in an individual to address the deficiencies and improve health and longevity. Nutraceutical and cosmeceutical products containing nanoencapsulated active ingredients are provided, in addition to dietary, exercise, sleep, and other lifestyle recommendations.
CN1969827A Anti-solid tumor composition containing epothilone and mesenchyme hydrolytic agent Disclosed is a pharmaceutical composition containing Epothilone and mesenchyma hydrolytic reagent characterized in that the pharmaceutical composition is in the form of slow release injection or slow release implanting agent, the slow release injection comprises slow release microspheres and dissolvent, the dissolvent being specific dissolvent containing suspension adjuvant. the mesenchyme hydrolytic reagent is proteolytic enzyme selected from collagenase, hyaluronidase, relaxin, plaxmin and blood vessel depressant selected from gefinitib, the Epothilone is selected from Epothilone B, Epothilone D, Isoepothilone D, the slow release auxiliary materials include polylactic acid and its copolymer, polyethylene glycol, PLA-COOH copolymer, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid), Polifeprosan, poly(lactic acid), biological compatible EVAc, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C) and is selected from sodium carboxymethylcellulose. When used for in-tumor or around-tumor injection or placement, the slow release agent can achieve and maintain medicinal concentration in the solid tumor, the effect for chemotherapy can also be improved.
CN1961867A Granule formulation of montelukast sodium The invention relates to a particle drug of Melusitena, wherein it comprises main components and assistant additive; the additive is the general additive used to prepare particle drug. The invention can avoid slow dissolvent, to make drug be absorbed fully. The invention can be used to treat asthma.
CN101366715A Rapamycin composition and preparation thereof The invention discloses a preparation composition containing rapamycin. The composition comprises an active ingredient the rapamycin, a solubilizer and a solid excipient, wherein the active ingredient the rapamycin and the solubilizer are dispersed into the solid excipient to form semisolid or solid dispersed substances. The rapamycin preparation composition has the characteristics of good stability, high absorptivity, simple technology of the preparation and the like, and not only can reduce the clinical medicine dosage, reduce the production cost, improve the clinical untoward reaction, reduce the individual difference of taking medicine but also can lighten the burden of patients and increase the compliance of taking medicine.
CN102702001A Stable amorphous ambroxol hydrochloride compound The invention belongs to the technical field of medicine, and particularly relates to an amorphous ambroxol hydrochloride compound and a preparation method thereof. The amorphous ambroxol hydrochloride compound has high purity and stability, does not have obvious moisture absorption and weight increase even under the condition of high humidity, ensures that relative substances do not grow, and has higher dissolution rate than crystalline ambroxol hydrochloride. The invention also relates to an application of the amorphous ambroxol hydrochloride compound in preparation of medicine for the treatment of acute and chronic pulmonary diseases with the symptom of ropy sputum and difficult expectoration, phlegm eliminating treatment of acute exacerbation of chronic bronchitis, asthmatic bronchitis and bronchial asthma, prophylactic treatment of lung complication after an operation, and treatment of infant respiratory distress syndrome (IRDS) of premature infants and neonates.
WO2014081324A1 Pyridyl hydrazones for the treatment of tuberculosis and related diseases The invention provides pyridyl-hydfazones of Formula I, or pharmaceutically acceptable salts, esters, solvates, isprriers and prodrugs thereof as well as pharmaceutical compositions containing these compounds for use in the prophylactic and/or therapeutic treatment of tuberculosis and related diseases, such as, diseases caused by nontuberculous mycobacteria and/or caused by Micobacterium leprae.
CA2338728C Pharmaceutical composition for injection based on paracetamol A pharmaceutical composition, characterized in that: a) it comprises i) paracetamol, ii) from 1 to 4 parts by volume of a low molecular weight alcohol for each part by weight of paracetamol, and iii) from 1 to 5 parts by volume of a polyethylene glycol for each part by weight of paracetamol; b) it is substantially anhydrous; and c) it forms a clear solution for injection with 4-10 parts by volume of water for each part by weight of paracetamol.
US8426428 EGFR kinase knockdown via electrophilically enhanced inhibitors Provided herein are electrophilically enhanced kinase inhibitors of Formula I. Also provided herein are methods of making and utilizing the same.
WO2014094840A1 Use of pidotimod to treat psoriasis The present invention is directed to the use of pidotimod, or a physiologically acceptable salt thereof, to treat psoriasis. For the treatment of the present invention, pidotimod, or a physiologically acceptable salt thereof, may be administered either systemically or topically.
CN101129385A Ophthalmic composition containing gatifloxacin and lotepredenol etabonate and method of preparing the same The invention discloses a turbid liquor eye composition with chlotiponuo and jiatishaxing and making method, which comprises the following parts: (a) 0. 2-2% chlotiponuo and salt with grain size below 50um, (b) 0. 2-1% jiatishaxing and salt, (c) 0. 5-2. 5% one or more non-ion polymer as suspension-assisting agent, (d) eye excipient agent. The making method comprises the following steps: grinding the chlotiponuo carbonate below 50um; sterilizing; adding jiatishaxing, non-ion polymer and other eye adjuvants to form an eye agent to treat and prevent opthalmitis and bacterial infection.
US20120245171 Benzpyrazole derivatives as inhibitors of pi3 kinases The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
WO2011161235A1 Semuloparin for use as an antithrombotic treatment in hip replacement surgery with improved safety in terms of clinically relevant bleedings The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof as an antithrombotic treatment in patients undergoing hip replacement surgery, wherein said use involves an improved safety in terms of clinically relevant bleedings and of major bleedings compared to a standard antithrombotic treatment.
CN103623106A Pharmaceutical foot bath composition for treating beriberi The invention discloses a pharmaceutical foot bath composition for treating beriberi. The pharmaceutical foot bath composition specifically consists of the following raw material medicines in parts by weight: 15-20 parts of alums, 15-20 parts of wild peppers, 7-10 parts of mints, 3-5 parts of Vb1, 3-5 parts of Vc and 100-200 parts of white vinegar. The pharmaceutical foot bath composition disclosed by the invention is easily available, low in cost, free from side effect and capable of effectively treating beriberi.
EP2613790A1 Laxative containing polyethylene glycol and electrolytes The invention relates to a laxative with improved compliance, containing polyethylene glycol (PEG). A medicinal product according to the invention is suitable for treating chronic obstipations and is characterized in that it comprises two components, A and B, which are spatially separated from one another, component A comprising a polyethylene glycol (PEG) and component B comprising at least one electrolyte.
CN101361771B Compound paclitaxel-oleum fructus bruceae injection emulsion and preparation method thereof The invention relates to a compound paclitaxel, namely oleum fructus bruceae emulsion for injection, and a preparation method thereof, which pertain to the field of medicine preparation, and aim at solving the technical problem of looking for a new paclitaxel emulsion for intravenous injection with large drug-loading rate, few side-effects and convenient drug administration and a preparation method thereof so as to meet the requirements of markets for the new medicine. Particularly, the new paclitaxel emulsion is prepared by the steps: after dissolving in ethanol, the paclitaxel is added withthe oleum fructus bruceae to form a compound oil phase and then is prepared into the emulsion of oil-in-water type with accessories for injection, such as lecithin, water for injection and the like. In the invention, the paclitaxel is obtained by a plurality of screening experiments; the paclitaxel in the compound oil phase consisting of ethanol and the oleum fructus bruceae has very high solubility; an external water phase does not contain the paclitaxel, and therefore the emulsion of oil-in-water type prepared effectively prevents phlebitis caused by the external water phase, greatly reduces anaphylactic reaction and enhances the adaptability of patients. In addition, the preparation of the emulsion has simple prescription and does not produce sediment after being diluted; embolizing does not occur during intravenous injection, thus providing a new paclitaxel emulsion for intravenous injection in clinical treatment.
CN101255154A Substituted 2-indoline ketone derivatives as well as preparation method and uses thereof The invention relates to a substituted 2-indolinone derivate, a preparation method and the applications thereof in antineoplastic. The substituted 2-indolinone derivate of the invention has a chemical general structure shown in the drawing, wherein X represents one of halogen and hydrogen, or nitro and alkoxyl; R1 and R2 are any one selected from hydrogen, alkyl, cycloalkyl, aryl and heteroary respectively; A represents any one of glycoside and isomer thereof, hydroxy and alkyl, and hydroxy and alkoxyl group. The substituted substituted 2-indolinone derivate of the invention generates nucleoside analogue of sunitinib by saccharification reaction or alkylation reaction of 2-indolinone, greatly increases the solubility, the antitumor activity and the virus resistance.
CN101138570A Multiple vitamin and mineral composition chewing tablet The invention relates to a health food product, in particular to a chewable tablet including a variety of vitamins and minerals applicable to pregnant women and lactating mothers. The ingredients include vitamin A, vitamin D, a vitamin B1, vitamin E, vitamin B2, vitamin B6, vitamin C, folic acid, pantothenic acid, anicotinamide, ferrous lactate, calcium carbonate, magnesium oxide, zinc lactate, sodium selenite, sugar, lactose, cocoa, mannitol, dextrin and magnesium stearate. Due to advanced dry granulation technology and GMP scale production, the invention completely avoids the loss of vitamin in the production process and ensures sanitary quality, safety and reliability, good taste, convenient use and low price of products.
US7745639 Dihydropyrazoles; anticarcinogenic agents can be synergistically combined with one or more active ingredients; side effect reduction The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
US20100221328 Sustained-release formulations Described herein are extended-release or sustained-release formulations suitable for highly soluble pharmacologically active compounds, for example, amantadine. Dosage units for providing extended release are provided by the present invention. In some embodiments, the dosage unit comprises a plurality of coated beads having drug layer and a coating layer, wherein the coating layer comprises an ethylcellulose polymer. In some embodiments, near zero-order release of the active compound is achieved.
CA2529293A1 Cyclopropyl group substituted oxazolidinone antibiotics and derivatives thereof This invention relates to new oxazolidinones, having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosisand other mycobacterial species. The compounds are represented by structural formula (I) its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.
CN103372015A Pessulum preparation containing drospirenone or drospirenone and estrogen The invention relates to a contraceptive which is a pessulum preparation containing drospirenone or drospirenone and estrogen. The pessulum comprises a controlled release membrane and one or more framework sections; and at least one framework section contains the drospirenone which can slowly release acyeterion at a constant speed within 21 days, so that the zero-order release characteristic is realized. The controlled release medicinal preparation containing the drospirenone or drospirenone and estrogen can overcome the inconvenience caused by an oral contraceptive pill and improve the compliance in taking the medicine.
EP1495014B1 Flavanoids derivatives as chemotherapeutic, chemopreventive, and antiangiogenic agents Novel compounds useful as chemotherapeutic, chemopreventive, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones. The compounds have the structure of formula (I), wherein R1 through R3 and R5 through R11 are defined herein, and α, β and Ϝ are optional bonds, providing that when α is absent, β is present, and when β is absent, α is present. When α is present, preferred R4 moieties are selected from O, S, NH and CH2, and when α is absent, preferred R4 groups are selected from OH, SH, NH2 and CH3. When Ϝ is present, the preferred R5 substituent is O, while when Ϝ is absent, the preferred R5 substituent is OH. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
US20130101565 Use of carbonic anhydrase ii for producing a drug The present invention falls within the field of biomedicine. Specifically, the present invention relates to the use of carbonic anhydrase II for the manufacture of a medicament for the prevention and/or treatment of the damage caused by ischemia, ischemia followed by reperfusion or toxins, acute failure or rejection of a transplanted organ, preferably the kidney. In a preferred embodiment, the toxin is cisplatin.
US20110288061 Triterpenoid derivatives, benzenoid derivatives and pharmaceutical compositions containing the same The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II): wherein, R1, R2, R3, R4, R5, R6, R7, R8, R1′, R2′, R3′, and R4′ are defined the same as the specification.
US20090069396 Polyene Oxazoles and Processes for Their Preparation This invention relates to novel biologically active polyene oxazoles, their pharmaceutically acceptable salts and derivatives, and to methods of obtaining them. One method for obtaining the compounds is by cultivation of Streptomyces sparsogenes NRRL 2940 or a mutant or variant thereof.
CA2752421C Amino ester derivatives, salts thereof and methods of use The present invention provides amino ester compounds, salts, and pharmaceutical formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating inter-and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
CN101486975B Streptomycete, method for producing tacrolimus using the same and use thereof The invention discloses a new streptomycete, a method that prepares tacrolimus by cultivating the streptomycete and application of the method. The Streptomyces sp.T300 (CGMCC1779) is a brand new strain and does not generate noxious H2S in a fermentation process. The streptomycete in a nutritious culture medium that has assimilable carbon and nitrogen sources and under the condition of being introduced with oxygen can be used for preparing the tacrolimus by fermented cultivation and can be applied into the preparation of tacrolimus-containing pharmaceutical compounds.
WO2014026073A1 Compositions with increased stability for inhibiting transient receptor potential ion channel trpa1 This disclosure describes solid forms of the compound of Formula (I) and pharmaceutical compositions for inhibiting the TRPAl ion channel and/or medical conditions related to TRPAl, such as pain.
WO2006130500A8 Tigecycline and methods of preparing 9-aminominocycline Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
US20120164226 Compositions and Methods for Improving Prognosis of a Human with Subarachnoid Hemorrhage The described invention provides a pharmaceutical composition, delivery system and a method for treating a delayed complication associated with a brain injury in a mammal and improving its prognosis in a mammal by implanting a therapeutically effective amount of the pharmaceutical composition containing a voltage-gated calcium channel blocker and a pharmaceutically acceptable carrier into a predetermined location in the brain, which reduces signs or symptoms of at least one delayed complication associated with brain injury.
US20100087467 Compositions Useful As Inhibitors of Protein Kinases The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein A, B, Q, R1, and R2 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT or PDK1 kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds, and methods of utilizing those compositions in the treatment of various disorders.
CN101262783A Nutritional supplement for a category of HIV patients The present invention relates to a nutritional product for HIV patients that are not on highly active antiretroviral therapy. More specifically the invention relates to a nutritional composition comprising oligosaccharides. This invention also relates to the manufacture of a nutritional supplement for use in HIV patients.
CA2781821A1 Processes for the preparation of deferasirox, and deferasirox polymorphs The present invention relates to processes for the preparation of deferasirox, an oral iron chelator developed to treat iron overload due to e.g. multiple blood transfusions. The present invention further provides novel deferasirox pseudopolymorphs and a novel amorphous form of deferasirox, processes for their preparation, as well as pharmaceutical compositions comprising same, and use thereof in treating iron overload.
US20110294890 Neramexane for the treatment or prevention of inner ear disorders The present invention relates to a method of treatment or prevention of an inner ear disorder in a female comprising administering a therapeutically effective amount of neramexane or a pharmaceutically acceptable salt thereof to a female.
EP1775303A1 Topiramate and pharmaceutical compositions thereof Topiramate (2,3:4,5-bis-O-(1-methylethylidene)-beta -D-fructopyranose sulfamate) in high-purity form, comprising at least 90% of particles with a size of 250 mu m or less, is new. An independent claim is also included for a pharmaceutical formulation comprising topiramate as above. - ACTIVITY : Anticonvulsant. - MECHANISM OF ACTION : None given.
US20120077827 Zap-70 active compounds Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on one or more protein kinases, including a Zeta-chain-associated protein kinase 70 (ZAP-70), and any mutations thereof.
CN101185626A Marimastat sustained-release implant for treating solid tumor A marimastat sustained release implant for treating solid tumors is characterized in that the sustained release implant includes effective dose of anticancer marimastat, sustained release excipients and a certain quantity of sustained release moderator. Solid tumors include pancreatic cancer, lung cancer, liver cancer, breast cancer, cerebroma, ovarian cancer, prostatic carcinoma, esophageal carcinoma, lymphadenoma, osteosarcoma and colorectal cancer. Sustained release excipients are mainly copolymer of glycolic acid and hydroxyacetic acid and one or combination of the multipolymer of glycollic acid and hydroxyacetic acid, polifeprosan, poly(L-lactide-co-ethyl phosphate), poly (L-lactide-co- phosphoric acid propyl); in the process of decompression, marimastat can be slowly released to local tumor, thus maintaining effective drug concentration in the local tumor as well as significantly reducing overall toxic reaction. Being placed in local tumor, the sustained release implant not only reduces overall toxic reaction of marimastat, but also selectively improves drug concentration in local tumor, enhancing the therapeutic effects of non-operative therapy such as chemotherapy drugs and radiotherapy.
US7449537 Antineoplastic polyalkoxyalkylsiloxanes and methods of use thereof Polyaminofunctional alkoxy polysiloxanes which exhibit antineoplastic activity are disclosed. Pharmaceutical compositions including an effective amount of a polyaminofunctional alkoxy polysiloxane and/or a pharmaceutically acceptable salt thereof are also disclosed. The application also describes methods of suppressing the growth of neoplastic cells and treating neoplastic conditions.
EP2088148A2 "Process for the preparation of solifenacin" A process for the preparation of (1S,3'R)-quinielidin-3'-yl-1-phenyl-3,4-dihydro-1H-isoquinolin-2-carboxylate, namely solifenacin, comprising the reaction of a compound of formula (IV) with a compound of formula (V), as herein defined, and the subsequent reaction with 3-quinuclidinol.
WO2013051562A1 Mouse mating inducer, mouse mating promotion method, and rodent trapping method At least one of the following, extracted from components contained in the urine of a female mouse in which estrus was induced by the administration of estrogen after an ovariectomy, is used: 2-ethylhexanol, undecane, and 2,3-butanediol diacetate. Applying these components to a female mouse increases pursuit behavior by male mice. Since no increases in pursuit behavior are seen in male mice from which the vomeronasal organ has been removed, the abovementioned components are pheromone-like substances that induce mating by way of the vomeronasal organ. These components are useful as mating inducers.
CN102784395A Application of MAPK-ERK1/2 signal channel inhibitor to preparation of double-minute medicine for removing or inhibiting tumor cells The invention discloses application of a MAPK-ERK1/2 signal channel inhibitor to the preparation of double-minute medicine for removing or inhibiting tumor cells and belongs to the technical field of tumor biological treatment. By aiming at the poor tumor treatment effect in the prior art, a target biological treatment strategy of tumors containing double minutes is further provided, the fact that double minutes in malignant cells and the ERK1/2 protein kinase activity have the close relationship obtained through research is used as the theoretical basis, and the application disclosed by the invention is specially provided by aiming at the ERK1/2 protein kinase continuous phosphorylation double-minute tumor type caused by the MAPK-ERK1/2 signal transduction channel abnormity. The method disclosed by the invention has the advantages that the tumor treatment specificity is improved, the existing treatment scheme is improved, and on the other hand, the invention also provides a strategy for double-minute targeting treatment.
CN101028252A Injection acetylcysteine powdery medicinal composition and its making method An acetylcysteine composition in the form of powder injection with high solubility and stability is prepared from acetylcysteine and pH regulate chosen from sodium dicarbonate, sodium carbonate, sodium hydroxide and bisodium dicarbonate in weight ratio of 1: (0.25-1). Its preparing process is also disclosed.
WO2010124623A1 Medicine for preventing and treating alzheimer's disease and preparative method thereof The present invention discloses a medicine for preventing and treating Alzheimer's disease, wherein the effective constituent is quercetin-3-O-β-D-xylopyranosyl-(l→2)-β-D-galactopyranoside (RNFG) extracted from Panax Notoginseng RNFG has estrogenic activity, antioxidant activity and protecting effect on nerve by preventing the assembly and toxicity of Aβ. RNFG also can decrease memory injury induced by scopolamine, and can be used in the manufacture of medicaments and health care products for preventing and treating Alzheimer's disease.
US20100331269 Triterpenes derivatives and uses thereof as antitumor agents or anti-inflammatory agents A compound of formula (I): wherein R1 is selected from the group consisting of H, α-L-Rhamnopyranose, α-D-Mannopyranose, β-D-Xylopyranose, β-D-Glucopyranose, and α-D-Arabinopyranose; R2 is selected from CH3, COOH, CH2OH, COOCH3 and CH2O-α-D-Arabinopyranose; with the proviso that the compound of formula (I) is not a compound of formula (I) wherein R1 is β-D-Glucopyranose and R2 is COOH; wherein R1 is α-L-Rhamnopyranose and R2 is CH3; wherein R1 is β-D-Glucopyranose and R2 is CH2OH; wherein R1 is β-D-Xylopyranose and R2 is CH2OH; wherein R1 is α-L-Rhamnopyranose and R2 is COOCH3, wherein R1 is H and R2 is CH3; wherein R1 is H and R2 is CH2OH; wherein R1 is H and R2 is COOH; or wherein R1 is H and R2 is COOCH3, or a pharmaceutically acceptable salt thereof.
US20080279866 Treating lymphomas, allergies and autoimmune diseases via apoptotic induction; using ATP-competitive inhibitor, 2-morpholin-4-yl-6-thianthren-1-yl-pyran-4-one (KU-55933) and lymphocyte specific immunoglobulins The present invention is directed to methods of inducing immunosuppression in a patient by administering an inhibitor of the enzyme Ataxia telangiectasia mutated (Atm). The method may be used as a treatment for allergies, autoimmune diseases or lymphomas. It may also be used to prevent organ rejection in transplant patients and to treat or prevent graft versus host disease.
US7220867 Dissolving with crystal growth inihibitos; drying The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib or a celecoxib drug substance of the invention in intimate association with one or more crystallization inhibitors, for example polymers. Also provided is a pharmaceutical composition comprising such a celecoxib-crystallization inhibitor composite and one or more excipients. Also provided are processes for preparing amorphous celecoxib, a celecoxib drug substance of the invention, a celecoxib-crystallization inhibitor composite of the invention, and a pharmaceutical composition of the invention. Also provided is a method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising administering, for example orally, a composition of the invention in a therapeutically effective amount.
CN103705461A Lipid microsphere preparation and preparation method thereof The invention provides a lipid microsphere preparation comprising propofol, flurbiprofen ester, oil phase solvent and emulgator. The invention also provides a method for preparing the lipid microsphere preparation. The method comprises the following steps: (1) mixing an oil phase mixture containing the propofol, the flurbiprofen ester, the oil phase solvent and the emulgator to generate uniform oil phase; (2) adding the oil phase to water phase to form colostrum; (3) homogenizing the colostrums. The lipid microsphere preparation is used as a dope and has improved abirritation simultaneously.
CN101065121A Therapeutic or preventive composition for gastric mucosa disease A method and apparatus for controlled charging of photoluminescent materials are provided. The method involves receiving a signal associated with an operating property of a luminescent system and determining if the signal satisfies an operating criterion. Electromagnetic energy is provided to the photoluminescent material until an ambient light level in proximity to the system exceeds a predefined level. The system includes a photoluminescent material and a sensor for detecting an operating property of the luminescent system. The system includes a control module for selectively illuminating the photoluminescent material based on the operating property until the ambient light level in proximity to the luminescent system exceeds a predefined level.
US20110008412 Oral Formulations for 5-HT-Receptor Agonists, Uses and Methods of Treatment Employing The Same A pharmaceutically acceptable oral formulation comprising core material which comprises a therapeutically effective amount of a 5-HT-receptor agonist, or a pharmaceutically acceptable salt, solvate or derivative thereof, which core material is provided with a substantially water resistant coating comprising one or more substantially water resistant materials.
US20100260811 Novel compositions of fat-soluble substances The invention relates to novel powderous, water-soluble compositions of fat-soluble substances and aqueous solutions or emulsions thereof, wherein the fat-soluble substance(s) are encapsulated as inner (discontinuous phase within an outer (continuous) phase of a matrix substance.
US20120039868 Biomarkers for Graft Rejection Methods are disclosed for diagnosing rejection in a transplanted subject, monitoring rejection in a transplanted subject at risk thereof, preventing, inhibiting, reducing or treating rejection in a transplanted subject, or identifying agents for use in the prevention, inhibition, reduction or treatment of rejection, based on genes which are differentially expressed in transplanted subjects.
CN1895375A Extracts of flaccid anemone and use thereof An extract of flaccid anemone rhizome used to prepare the medicines for treating rhumatoid diseases contains the general triterpenoid saponin (more than 30%).
US20080194636 Controlling insulin aminiopeptidase; cognition activators; induction labor and lactation; side effecxt reduction The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions, regulating cellular glucose uptake and homeostasis, inducing labour and lactation, and other disorders or conditions wherein excessive or undesirable IRAP activity is implicated.
CA2849218A1 Compositions and methods for treating disorders associated with overweight animals The invention encompasses compositions and methods for treating disorders and diseases associated with overweight. The application also encompasses genes differentially expressed in animals and particularly to genes differentially expressed in overweight animals compared to lean animals.
WO2010022196A2 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase The present invention is directed to an indole benzylamine compound useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient a therapeutically effective amount of the compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier. Formule (I).
US20090004295 Use of a chemically-stabilized chlorite solution for inhibiting an antigen-specific immune response Methods of using a stabilized chlorite solution to inhibit antigen-specific immune responses are disclosed. The stabilized chlorite solution, when administered to a mammal in need thereof, can prevent the presentation of antigens by antigen presenting cells. The stabilized chlorite solution therefore is useful in treating, inter alia, auto-immune diseases, treating diseases caused by an inappropriate immune response, treating lymphoproliferative disease and in inhibiting rejection in transplant patients.
EP1282619B1 Processes for the preparation of thiazolidinedione derivatives and intermediates The present invention is concerned with a novel process for the preparation of compounds of formula (I) comprising bromomethylation or chloromethylation of a compound of formula (II) and subsequent reaction with a compound of formula (III). The compounds of formula (I) and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances.
US20080138421 And a stabilizer of xylitol, sorbitol, polydextrose, isomalt, dextrose; gel matrix; urinary incontinence, urinary urge incontinence, imperative urinary urge, and/or increased urinary frequency The present application relates to a pharmaceutical granulate comprising Fesoterodine or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable stabilizer, which can be selected from the group consisting of sorbitol, xylitol, polydextrose, isomalt, dextrose, and combinations thereof, and is preferably a sugar alcohol selected from the group consisting of xylitol and sorbitol. The granulate is suitable for incorporation into pharmaceutical compositions comprising a gel matrix formed by at least one type of hydroxypropyl methylcellulose into which the Fesoterodine is embedded and, optionally, further excipients. In certain embodiments, the granulate is formed by a process of wet granulation.
CN102875689A Preparation method and application of ophiopogon japonicus polysaccharide The invention relates to an ophiopogon japonicus polysaccharide and a preparation method thereof. The method includes selecting dwarf lilyturf tuber, subjecting the dwarf lilyturf tuber to ethanol extraction, water extraction and ethanol precipitation, taking precipitates by centrifugation to obtain the ophiopogon japonicus polysaccharide, taking a crude polysaccharide, dissolving the crude polysaccharide with water, adding activated carbon for boiling, subjecting the crude polysaccharide to membrane separation, ethanol precipitation and centrifugation, taking precipitates, and drying the precipitates to obtain the ophiopogon japonicus polysaccharide. The method for producing the ophiopogon japonicus polysaccharide has the advantages of being reliable in techniques, simple in operating steps, controllable in conditions and suitable for large scale production. The distribution ranges of molecular weight of the prepared ophiopogon japonicus polysaccharide is fixed, the weight-average molecular weight is smaller than 5000 dalton, the total polysaccharide content reaches 90%, and ophiopogon japonicus polysaccharide injection prepared by using the ophiopogon japonicus polysaccharide is capable of enhancing immunity and inhibiting tumors.
CN102844315A Crystalline salts of a potent hcv inhibitor This invention relates to novel tris(hydroxymethyl)aminomethane, choline and N-methyl-D-glucamine salt forms of the following Compound (1) and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection.
WO2008036277A1 Pyraz0l0(l,5-a) (1, 3, 5) triazine and pyrazolo (1, 5-a) pyrimidine derivatives useful as protein kinase inhibitors Pyrimidine- and triazine-based chemical compounds having the structure (I) that are useful, for example, as protein kinase inhibitors for treating cancer, neurological disorders, autoimmune disorders, and other diseases, and methods of using such compounds.
CN1648126A Compound and its preparing method and use The present invention provides one new compound in the structural expression as shown in (I). The compound is separated from dry flower of Trollius chinensis Bunge, Trollius asiaticus L., Trollius farreri Stapf, Trollius ledebouri Reichb or Trollius macropetalus Fr. Schmidt. The compound has powerful antiseptic and antiviral activity and antitumor activity. The present invention also provides the preparation and use of the compound.
US20100173779 Composition and method to stimulate growth and defense against pathogens in plants An aqueous composition to stimulate growth and defense against pathogens and other favorable productive properties in plants, including an oligo-carrageenan selected from kappa 1, kappa 2, lambda or iota oligo-carrageenans. Also, a method of spraying said the composition over the leaves of the plants and its use to stimulate defense against tobacco mosaic virus (TMV) and increase the height, the foliar biomass and the number of leaves in a plant. Also including a preparation method of the composition.
US20080242599 Compositions and Methods for Increasing Osteoblast Cell Differentiation and Bone Generation The present invention relates to the discovery of a novel pathway for the induction of osteoblast cellular differentiation and bone generation. Specifically, the present invention envisions a novel screening tool for the determination of compounds capable of promoting osteoblast cellular differentiation that could be used in the treatment of various bone-loss or bone density decreasing disorders. The method of screening of the present invention enables one to determine whether a compound affects certain pathways that promote via direct induction, or the downregulation of inhibiting activity, the differentiation of progenitor cells into osteoblasts. This promotion of osteoblasts could provide for treatments for bone-loss or bone density disorders. The invention further encompasses methods of increasing bone density using the compounds, the compounds, and pharmaceutical compositions comprising the compounds.
US20120277212 Novel Oxime Derivatives and Their Use As Allosteric Modulators of Metabotropic Glutamate Receptors The present invention provides new oxime derivatives of the general formula (I), pharmaceutical compositions containing them and their use for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. This invention further provides new oxime derivatives of the general formula (I) consisting of modulators of nervous system receptors sensitive to glutamate, which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. In particular embodiments, the new oxime derivatives of the invention are modulators of metabotropic glutamate receptors (mGluRs). The invention further provides positive allosteric modulators of mGluRs and more specifically positive alSosteric modulators of mGluR4.
CN103182042A Plaster for treating mumps, and preparation method thereof The invention belongs to the technical field of medicine, and in particular relates to a plaster for treating mumps, and a preparation method thereof. The effective components of the plaster for treating mumps comprises the following raw materials in parts by weight: 14-22 parts of rhubarb, 14-22 parts of frankincense, 14-22 parts of burreed tuber, 14-22 parts of achyranthes root, 14-22 parts of spatholobus stem, 14-22 parts of safflower, 14-22 parts of dragon's blood, 14-22 parts of black catechu, 12-20 parts of garden balsam seed, 7-13 parts of snake slough, 7-13 parts of carbonized hair, 25-35 parts of pagpdatree flower, 450-550 parts of minium and 950-1050 parts of ground sesameseed oil. The plaster has the effects of reducing swelling, reducing fever and relieving pain, is used for external treatment of mumps, has reliable curative effect, and avoids the difficulties in oral administration in children and drug injection.
US20100202973 Microrna molecules associated with inflammatory skin disorders This invention relates to the finding that inflammatory skin disorders, such as psoriasis and atopic eczema, are characterized by changes in the expression of specific microRNA molecules (miRNAs). These miRNAs may therefore be useful as biomarkers for inflammatory skin disorders as well as therapeutic targets. Methods of diagnosis and treatment of inflammatory skin disorders are provided, as well as methods of screening for therapeutic compounds.
WO2009073148A3 Polymorphs of n-malonyl-bis(n'-methyl-n'-thiobenzoylhydrazide) At least 70% by weight of Compound 1 is the single crystalline form, Form A, Form C, or Form D, of the compound. A pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent, and compound 1, wherein at least 70% by weight of the compound is the single crystalline form, Form A, Form C, or Form D, of the compound. A method of treating a subject with cancer comprises administering to the subject an effective amount of compound 1 or the pharmaceutical composition.
CN102641272A Medicament composite of methionine vitamin B1 and preparation method of the medicament composite The invention relates to a medicament composite of a methionine vitamin B1. The medicament composite contains the following ingredients in parts by weight: 10 parts of methionine, 1 part of vitamin B1, 30 parts of mannitol, 2-5 parts of povidone K30 and 0.05-0.2 part of thioglycerol. Mannitol, povidone K30 and thioglycerol are adopted as adjuvants, wherein mannitol is taken as excipient and medicament stability is improved by povidone K30 and thioglycerol. The combined use of povidone K30 and thioglycerol has an unexpected remarkable effect for the improvement of the medicament stability. By povidone K30, the dissolubility of impurities possibly generated by the degradation of thioglycero and the medicament is increased and the heat stability of the medicament is enhanced.
US20050123983 Methods and compositions for overcoming resistance to biologic and chemotherapy This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.
CN102838969A Ice slush and preparation method thereof The invention discloses ice slush, and solves the problems that in the prior art, ice is too hard and easily leads to mechanical damage to a user, the lasting cooling time is too short, and the use by the user is very troublesome. The ice slush is prepared from ethanol, borneol, vaseline, salt and water. The invention also provides a preparation method of the ice slush. According to the invention, the ice slush maintains to be in a soft state all the time, does not have any damage to the human body, and is good in refrigeration effect.
US20100136106 Modified Release Famciclovir Compositions The invention relates to a multiparticulate modified release composition that, upon administration to a patient, delivers famciclovir in a bimodal, multimodal or continuous manner. The multiparticulate modified release composition comprises a first component and at least one subsequent component, the first component comprising a first population of active ingredient containing particles and the at least one subsequent component comprising a second population of active ingredient containing particles. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition, and to a method for the treatment or suppression of viral infections.
WO2007034316A1 Process for annealing amorphous atorvastatin Processes for annealing amorphous atorvastatin is described. Pharmaceutical compositions and formulations containing annealed amorphous atorvastatin are also described.
EP1913944A1 Pharmaceutical combinations and their use in treating gastrointestinal disorders The present invention relates to a combination of a first agent inducing either a 5-HT4 receptor agonist or antagonist or a 5-HT3 receptor antagonist and a co-agent and pharmaceutical compositions and formulations containing the combination. The pharmaceutical combination may be employed for the treatment of altered gastrointestinal motility, sensitivity, secretion or abdominal disorders. The dosage is preferably oral. The preferred first agent is tegaserod.
US20120004313 Crystalline form vi of agomelatine, preparation method and application thereof The invention provides a new crystalline form of agomelatine, preparation and use thereof. The X-ray powder diffraction diagram of the agomelatine crystalline form shows main peaks at the diffraction angles 2θ 11.13°, 11.82°, 17.49°, 18.29°, 19.48°, 19.72°, 20.50°, 21.76°, 22.54°, 22.97°, 24.56°, 25.36°, 27.16° and 31.93°. Said new crystalline form is characterized by high purity, stability and good reproducibility, and thus is advantageous for the pharmaceutical formulation. In addition, the stability and solubility of said crystalline form are also superior over the several existing crystalline forms.
WO2006035796A1 1-(β-D-GLYCOPYRANOSYL)-3-SUBSTITUTED NITROGENOUS HETEROCYCLIC COMPOUND, MEDICINAL COMPOSITION CONTAINING THE SAME, AND MEDICINAL USE THEREOF A compound having SGLT1 and/or SGLT2 inhibitory activity which is usable as a preventive or therapeutic agent for diabetes, postprandial hyperglycemia, impaired glucose tolerance, complications of diabetes, obesity, etc. It is a 1-(β-D-glycopyranosyl)-3-substituted nitrogenous heterocyclic compound represented by the general formula (I), a prodrug or pharmacologically acceptable salt thereof, or a hydrate or solvate of either. Also provided is an SGLT inhibitor containing any of these. [In the formula, ring A represents optionally substituted aryl or heteroaryl; Q1 to Q5 each independently represents either a carbon atom having a hydrogen atom or substituent bonded thereto or a nitrogen atom; E represents a single bond, alkylene, -O-, -S-, or -NH-; and R represents methyl, ethyl, fluoromethyl, or hydroxymethyl.]
US20120232137 Use of Bethaneciol for Treatment of Xerostomia Bethanechol is administered topically, for the treatment of xerostomia.
CN101239925A Method for preparing magnesium aspartate Provided is an sspartic acid magnesium preparing method belonging to the chemical field, which is characterized in that, magnesium salts and sspartic acid are added in water so that partial or whole moisture is removed after reaction, the remains is added in a water soluble non-aqueous solvent to separate out solid, and the product is obtained through crushing and drying. Compared with the prior art, the invention has advantages of improved yield, reduced production cost, increased production efficiency and product quality.
US20060122241 Novel macrocycles for the treatment of cancer diseases The present invention relates to novel macrocycles of the general formula (I) and to the use thereof in the treatment of cancer diseases.
WO2014009779A1 Selective inhibition of the membrane attack complex of complement and c3 convertase by low molecular weight components of the aurin tricarboxylic acid synthetic complex Selective inhibition of the membrane attack complex of complement in a mammalian species, preferably human, with components of the aurin tricarboxylic acid complex of less than 1 kilodalton in molecular weight. Preferred inhibitors are aurin tricarboxylic acid, aurin quadracarboxylic acid and aurin hexacarboxylic acid. Preferred disease to be treated by elective inhibition of the membrane attack complex of complement are age-related macular degeneration, Alzheimer's disease, atherosclerosis, rheumatoid arthritis, paroxysmal nocturnal hemoglobinemia, malaria infection and multiple sclerosis.
EP1102753B1 Pyrazoles as estrogen receptor modulators Estrogen receptor-modulating pyrazole compounds are described in addition to methods and compositions for treating or preventing estrogen receptor-mediated disorders. The compounds described have been found to have unexpected and surprising activity in modulating estrogen receptor activity. Thus, the compounds of the present invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
WO2012054792A2 Composition and method for immunological treatment of cancer, prevention of cancer recurrence and metastasis, and overcoming immune suppressor cells Methods for the ex vivo generation of cells of the innate (NKT cells and NK cells) and adaptive (T cells) immune systems for use in adoptive cell transfer (ACT) are provided. The NKT cells render T cells resistant to immune suppression (e.g. they are resistant to the effects of myeloid-derived suppressor cells (MDSCs)). The method involves culturing disease- primed immune cells (obtained from a cancer patient or from a patient with an infectious disease) with i) byrostatin and ionomycin (B/I) to activate and differentiate the cells; followed by sequentially culturing the cells with a) a combination of IL-7 and IL-15 and then b) IL-2, to further differentiate the cells and to render them immune resistant. The resistant immune cells are used to treat and prevent cancer and infectious diseases.
CN1923189A Taxine kind anti-cancer slow release injection The invention relates to a slow-release injection of taxine anti-cancer drug, which comprises anti-cancer drug, slow-release finding, suspension and/or solvent. Wherein, said anti-cancer drug is taxine, 2'-hydroxy Paclitaxel, etc; the slow-release finding is polymer of hydroxyl, glycollic acid and glycolic acid, one of acetic acid ethyenyl ester polymer and polyphony; the suspension is polyphenyl (sodium), and mannite; the solvent is distilled water, injection water, absolute ethyl alcohol, etc. The invention can be injected to reduce the toxicity effect of drug, and improve the density locally to strengthen the treatment effect of chemotherapy and radiation therapy.
CN1883456B Flavor-hidden pharmaceutical granule, preparation method and use thereof The invention provides taste-masked medicinal granules prepared through macromolecular blending method, the process for preparing the taste-masked medicinal granules and the use in preparing oral disintegrating tablets. The preparing process comprises mixing micronized active medicinal constituents with three medicinal macromolecular auxiliary materials for blending treatment, making complete sheet material and disintegrating, finally granulating to obtain the end particles.
CN102617698A Method for preparing fine dioscin and application of fine dioscin The invention relates to a method for preparing fine dioscin and an application of the fine dioscin to antitumor aspect. The preparation method comprises the following steps of: weighing medicinal materials, putting into an extracting tank, soaking the medicinal materials with a water-containing organic solvent of which the amount is 3-12 times (v/w) that of the medicinal materials for 30-100 minutes, heating to 40-100 DEG C, refluxing or extracting with other auxiliary methods for 1-8 hours, draining an extracting solution, and extracting for 2-5 times; concentrating and recovering the solvent, draining a residual liquid, standing, precipitating a precipitate out, filtering, and drying and smashing a filter cake to obtain a crude product; and repeatedly crystalizing the crude product with the solvent to obtain a pure product of which the purity is over 95 percent. As proved by results of in-vitro and in-vivo antitumor tests on the fine dioscin, the fine dioscin prepared with the method has an antitumor effect, and particularly has better effects on the aspect of inhibition of human intestinal cancers, human kidney cancers, human prostatic cancers and human mammary cancer tumor cells. The fine dioscin prepared with the method can be prepared into antitumor tablets, capsules, injections, oral liquids and the like.
US20110189195 Method for controlling cancer metastasis or cancer cell migration by modulating the cellular level of lysyl trna synthetase The present invention relates to a novel function of lysyl tRNA synthetase (KRS) which enhances tumor cell migration and affects cancer metastasis via KRS's interaction with laminin receptor (67LR) by its translocation to membrane. More particularly, the present invention relates to a method for modulating cancer metastasis or migration, which comprises regulating intracellular levels of KRS; a composition for preventing or treating cancer; use of expression vector for inhibiting the expression of KRS; a method for preventing or treating cancer; use of an agent for inhibiting an activity of KRS; a method for screening an agent which modulates cancer metastasis or migration; and a method for screening an agent which inhibits the interaction of KRS with 67LR, by said novel function. Thus, KRS can modulate cancer metastasis or migration and furthermore, can modulate intra-cellular metabolism related to 67LR. The interaction between KRS and 67LR can be used effectively in treating, preventing and/or diagnosing of various diseases or disorders related to the interaction.
CA2288143C Activated protein c formulations The present invention relates to pharmaceutical formulations of activated protein C which also comprises sucrose, sodium chloride and sodium citrate buffer at a pH between about 5.5 and about 6.5. The activated protein C formulations of the present invention are more stable than other formulations of activated protein C and demonstrate fewer degradation products over time.
US20080311090 Methods for inhibition of proliferative disease, including hepatocellular carcinoma The present invention is related to a method for modulating expression of protein kinase C-alpha associated with proliferative diseases. The invention further relates to a screening method utilizing the association between transcription factors (MZF-1 and Elk-1) and their DNA binding element (PKC-.alpha. promoter) to identify novel anticancer agents.
WO2012019439A1 Huperzine a ophthalmic microemulsion and preparation method thereof A Huperzine A ophthalmic microemulsion and preparation method thereof. The microemulsion is prepared with Huperzine A, an oil, an emulsifier, an osmotic pressure regulator, an ion-pair reagent, a thickening agent, an antioxidant, a metal chelator, an antibacterial agent, a pH regulator, and purified water, wherein the ion-pair reagent may be one or more types of sorbic acid and potassium sorbate.
US20100260865 Viricidal composition A non-staining composition which is bactericidal, fungicidal and viricidal when applied, comprising in combination; an iodine free bactericide and/or fungicide having a residual efficacy lasting longer than 3 hours on surfaces against bacteria and fungi and a peroxide. A carrier may also be present. The bactericide and/or fungicide may be for example triclosan or a quaternary ammonium compound, or preferably a PVP-phenolic biocide complex (eg PVP-triclosan) or PVAIc/quaternary ammonium compound complex (eg PVP/benzalkonium chloride). The peroxide may be hydrogen peroxide.
EP2108369A1 Compounds for the treatment of immunosuppression in the skin caused by aggressive agents The invention relates to 2,4-O-furfurylidenesorbitol or alkyl ethers thereof, for the treatment of immunosuppression in the skin caused by aggressive agents such as pollutants, dehydrating agents, ultraviolet rays, thermal and osmotic shock, and a pharmaceutical, dermatological, nutritional or cosmetic composition containing these, as is or in a mixture, as active principle.
CN103315978A Dry docetaxel elixir, and preparation method and application thereof The invention discloses a dry docetaxel elixir and a preparation method and application thereof. The preparation method comprises the following steps: adding an alcoholic solution of docetaxel into a solution of a capsule wall material at a speed of 10 to 20 mL/min drop by drop and then carrying out uniform mixing and spray drying, wherein the capsule wall material is one or more selected from the group consisting of chitosan, dextrin, gelatin and starch, the alcoholic solution of docetaxel comprises docetaxel and ethanol, a weight ratio of docetaxel to ethanol is 0.00125-0.0125: 1, and a weight ratio of docetaxel to the capsule wall material is 0.1-1.0: 1. The preparation method for the dry docetaxel elixir provided by the invention has simple process, is easy to operate and applicable to large scale production in the industry of preparations and can substantially improve solubility and bioavailability of docetaxel and compliance of a patient; and the prepared dry docetaxel elixir has the advantages of uniform particle size distribution, high drug loading capacity and encapsulation efficiency and fast drug release.
US20110218176 Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development The present invention relates to prevention of congenital deformations. The invention further relates to cancer inhibition and prevention. The invention further relates to methods and compositions to modulate, antagonize, or agonize disparate signaling pathways that may converge to regulate patterning events and gene expression during prenatal development, post-natal development, and during development in the adult organism. The invention also relates to activators or deactivators of pyruvate kinase M2 (PKM2) for the treatment, prevention, or amelioration of diseases related to PKM2 function.
CA2539033C Treatment of disease or injury of the nervous system with fty720 Methods for modulating neurogenesis in vitro and in vivo have been disclosed. The methods comprise contacting neural stem cells with an effective amount of a FTY720 compound. The neurogenesis may involve the modulation of proliferation, differentiation, migration or survival of a non-embryonic neural stem cells or progenitor cells. Also disclosed are methods for the prevention or treatment of neurological disorders including Parkinson's desease, Parkinsonian disorders, Hutington's disease, Alzheimer's disease, amyotrophic lateral sclerosis, spinal ischemia, ischemic stroke, spinal cord injury, cancer-related brain injury, and cancer-related spinal cord injury, Shy-Drager syndrome, progressive supranuclear palsy, Lewy body disease, stroke, cerebral infarction, multi-infarct dementia, and geriatric dementia, comprising administering to a subject a therapeutically effective amount of a FTY720 compound.
US7572791 Long-term stability, extended delivery using a suitable reservoir; pumped or metered at a controlled rate; implantable or external pump device, pen style injection device; stable at physiologic temperatures for duration of therapeutic exposure; supply of therapeutically active material for up to 2 years Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer; and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.
US20070032471 Active substance combination comprising a 2,5-dihydroxybenzenesulfonic compound and a potassium ion channel modulator The present invention relates to an active substance combination comprising at least one 2,5-dihydroxybenzenesulfonic compound and at least one K+ channel modulator, a medicament comprising said active substance combination, a pharmaceutical formulation comprising said active substance combination and the use of said active substance combination for the manufacture of a medicament.
WO2013149322A1 Preventing or treating periodontal disease The disclosure relates to a method for treating or preventing periodontal disease, such as gingivitis or periodontitis. The method may comprise providing an antimicrobial composition disposed within a reservoir, the reservoir being fluidly connected to an exterior surface of an applicator having a frictional stress value sufficient to cause mechanical displacement of a biofilm present on an oral cavity surface; dispensing said antimicrobial composition through said applicator onto said exterior surface of said applicator; applying the antimicrobial composition to the oral cavity surface; and rubbing said applicator onto said oral cavity surface and exerting pressure towards said oral cavity surface.
CN102988461A Rhodiola rosea injection and preparation method thereof The invention provides a rhodiola rosea injection and a preparation method thereof. The rhodiola rosea is prepared from a rhodiola rosea extract, vitamin B12, an auxiliary material and injection water. The preparation method of the rhodiola rosea injection comprises the following steps of: extracting a rhodiola rosea crude extract from a rhodiola rosea medicinal material; extracting the rhodiola rosea crude extract by using ethanol of which the volume percentage concentration is more than 90 percent, and refining the rhodiola rosea crude extract; refluxing the refined rhodiola rosea extract and the vitamin B12 by adding water, and filtering to obtain a rhodiola rosea extracting solution; and mixing the rhodiola rosea extracting solution with the auxiliary material to prepare the rhodiola rosea injection. By utilizing the preparation method, various impurities can be effectively removed, the effectiveness of the medicament is improved, the quality stability of the rhodiola rosea injection is improved, and the safety risk is reduced. The rhodiola rosea injection is high in active ingredient content, so that the curative effect is ensured, various impurities in the rhodiola rosea extract are reduced, and the quality stability of the rhodiola rosea injection is improved.
CN102531949A Substituted benzamide compounds and preparation method and application thereof The invention relates to substituted benzamide compounds shown as a general formula (I) or medicinal salts thereof, preparation of the compounds or the medicinal salts thereof, a medicament composition containing the compounds or the medicinal salts thereof and application of the compounds in treatment of cancers, in particular application in treatment of head and neck cancers, non-small cell lung cancer, pancreatic cancer, colorectal cancer, bladder cancer, breast cancer, ovarian cancer and flat cell cancer and application in medicaments for treating the cancers.
CN101185690A Medicine for preventing and overcoming climate sickness The invention relates to a medicine preventing and overcoming endemic, which mixes hawthorn powder or hawthorn pulp with fructo-oligosaccharide (FOS) serosity or powder according to scientific proportion, and stirs evenly; machines are used for squashing the mixture into tablets, globulus and pills, thus making into non-prescription health care medicine; the medicine is taken from 3 to 10 days before the travel till the seventh day at home after the travel is finished, and the purpose of preventing and overcoming climate sickness thus is achieved. The medicine can also be taken frequently at ordinary times for the sake of daily health care, which is also the requisite of military supplies of army camping trip and operation. The non-prescription health care medicine has no toxicity and side effects.
WO2011098262A2 P19arf, hmga2 and mdm2 for use in the diagnosis and treatment of aberrant cell growth Provided are novel methods and compositions for the diagnosis, prognosis and treatment of leiomyomas, in particular uterine leiomyoma (UL). In addition, methods of identifying antitumor agents are described. Furthermore, novel methods and compositions are provided for the treatment of diseases characterized by an aberrant growth of mesenchymal stem cells and their descendants and for the treatment of obesity are disclosed.
EP1743632A1 Novel 4-dedimethy laminotetracycline derivatives The present invention provides novel 4-dedimethylaminotetracycline compounds that are substituted at the 9 position and the use of said compounds for the manufacture of a medicament for the treatment of a mammal suffering from a condition that benefits from a non-antimicrobial dose of said compounds.
EP1688147A1 Methods Related to Immunostimulatory Nucleic Acid-Induced Interferon Methods and compositions are provided for extending the clinical utility of IFN-α in the treatment of a variety of viral and proliferative disorders. Among other aspects, the invention provides methods which increase the efficacy of IFN-α treatment and reduce IFN-α treatment-related side effects. In addition, methods are provides for supporting the survival and for activating natural interferon producing cells (IPCs) in vitro without exogenous IL-3 or GM-CSF. The invention is based on the discovery that certain CpG and non-CpG ISNAs promote survival and stimulation of IPCs.
US20100003309 Method for the production of fentanyl-based anesthetics for their oral transmucosal administration in a candy-like dosage form A method for the production fentanyl-based analgesics for their oral transmucosal administration in a candy-like dosage form, involving the dissolution of a pharmacologically accepted amount of Fentanyl citrate in purified water and the dissolution of a pharmacologically accepted dye in purified water. Mix polyalcohol sugar with purified water with a ratio polyalcohol/sugar between 17 and 19.5% by weight. Stir slowly over low heat until a liquid and smooth mass is obtained. Add sucrose to this liquid mass with a ratio liquid mass/sucrose between 65% and 67.5% by weight. Heat the mass and bring to a boil from an initial temperature of 128°-1320 C to a maximum temperature of 148°-152° C., until its water content evaporates and the weight of the mass obtained in this step reaches between 88% and 90% by weight with respect to the initial total weight of the liquid mass. Leave the mass to cool to a temperature of about 1280 C, and add the Fentanyl citrate solutions, the dye and flavouring agent, stirring firmly and maintaining the same temperature. Pour this hot mixture with a temperature of about 1300 C into a mould or matrix. Before the candy mass sets, a handle can be attached to each candy piece. When the mould is cold and the candy has solidified, remove from the mould and immediately wrap or bag the pieces.
EP2342335A1 Novel gene cluster Novel isolated DNA sequences which comprise all or part of a gene cluster encoding sanglifehrin synthase, processing and regulatory genes involved in the biosynthesis of a mixed non-ribosomal peptide/polyketide compound, or mutants having altered biosynthetic capability, polypeptides or mutants thereof encoded by DNA or the mutants, vectors containing the DNA or the mutants thereof, host cells transformed with the DNA, the mutants thereof, or the vector, and a method for producing sanglifehrin compounds. Compounds with cyclophilin inhibition activity used as immunosuppressants, antivirals or cardiac protection agents.
CN103505441A Oral solid preparation containing biguanides and acarbose and preparation method thereof The invention provides a method for preparing an oral solid preparation containing biguanides and acarbose. The method comprises the following steps: 1) pelletizing the biguanides and pharmaceutical acceptable auxiliary materials by a wet process, and obtaining dry biguanides granules in a drying manner; 2) directly mixing the dry granules prepared in the step 1) with the acarbose and the pharmaceutical acceptable auxiliary materials, so as to prepare the oral solid preparation. The invention also provides the oral solid preparation containing biguanides and acarbose prepared by the method.
CA2098176C Angiotensin ii receptor blocking compositions This invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier, an angiotensin IIreceptor antagonist and a second agent selected from a diuretic, a calcium channel blocker, a .beta.-adrenoceptor blocker, a renin inhibitor, or an angiotensin converting enzyme inhibitor and a method of treating hypertension.
US20080286209 Comprising isoprenoid-based compounds (e.g., farnesol and/or farnesol analogues or derivatives) or dehydroisoprenoid-based compounds, for use in treating (e.g., suppressing) alcohol withdrawal syndrome and associated neurological symptoms (e.g., depression, tremor, anxiety) Particular aspects of the present invention provide pharmaceutical compositions comprising isoprenoid-based compounds (e.g., farnesol and/or farnesol analogues or derivatives) or dehydroisoprenoid-based compounds, and novel methods for using same in treating (e.g., suppressing): alcohol withdrawal syndrome and associated neurological symptoms (e.g., depression, tremor, anxiety, autonomic hyperactivity (e.g., sweating, increased blood pressure, tachycardia), hallucinations, alcohol withdrawal seizures, delirium tremens (DT), and memory loss); or for treating in treating convulsive seizure (e.g., epileptic seizure, etc.). Particular pharmaceutical compositions and methods comprise the use of at least one compound selected from the group consisting of: (2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ol (all-trans farnesol); (2Z,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ol (cis-farnesol); (E)-3,7,11-trimethyldodeca-1,6,10-trien-3-ol nerolidol); (2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-amine (farnesylamine); (E)-3-(3,7-dimethylocta-2,6-dienyloxy)phenol (geranylresorcinol); (2E,6E)-,7,11-dimethyl-3-(trifluoromethyl)dodeca-2,6,10-trien-1-ol (trifluorofarnesol); and (2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-1-enyl)nona-2,4,6,8-tetraen-1-ol (all-trans retinol). According to additional aspects, compounds that target and inhibit enzymes that degrade/metabolize/inactivate the disclosed compounds have utility to induce endogenous accumulation thereof to suppress/prevent, e.g., alcohol withdrawal seizures or convulsive seizures.
CN102895542A Medicine for treating infant skin fold ulcer The invention relates to the field of infant skin care products, in particular to a medicine for treating infant skin fold ulcer and solves the problems that shortcomings exist in prior treating methods or medicines. The medicine is prepared by oat powders, oven earth powders and corn starches. The preparation method includes that oat seeds are subjected to screening, impurity cleaning and washing, then the oat seeds are subjected to sterilization and disinfection, the oat seeds are fried and baked to brown yellow, the impurity cleaning is performed again, scorched particles are removed, and finally the oat seeds are smashed to be powders to obtain the oat powders; loess blocks are placed in a stove, the stove is ignited by adding fuels, when the fire is naturally extinguished and the loess blocks are cooled, the loess blocks are taken out, burned black outer surface is removed through a knife to obtain fulvous oven earth, and the oven earth is smashed to be powders to obtain the oven earth powders; pure white corn starches are chosen; and the oat powders, the oven earth powders and the corn starches are subjected to sterilization and disinfection, the homogeneity is performed in proportion, then the sterilization and disinfection are performed again, and bagging is performed to obtain the medicine. The medicine for treating the infant skin fold ulcer has the advantages that the efficacies of stopping bleeding, astringing, activating cells, eliminating stasis, reducing swelling, eliminating necrotic tissues and promoting tissue regeneration are achieved, the compatibility of the medicine is reasonable, the medicine is natural and free of stimulation, functions of preventing infection and relieving pain are achieved, and simultaneously the application is simple and convenient.
CN1981771A Ointement for treating ringworm An ointment for treating skin tinea, especially the psoriasis, is prepared from dexamethasone acetate and aciclovir in the ratio of (0.75-4.50):30.
US20080280880 Staurosporine Derivatives for Use in Alveolar Rhabdomyosarcoma This invention relates to staurosporine derivatives are effective when used in combination with ionizing radiation for the delay of progression or treatment of a proliferative disease, especially a disease associated with a PAX/FKHR translocation including a PAX3/FKHR translocation and a PAX7/FKHR translocation, more especially a solid tumor disease such as a Sarcoma, most especially an Alveolar Rhabdomyosarcoma.
WO2012010938A3 Pharmaceutical composition of cefditoren pivoxil A pharmaceutical composition comprising cefditoren pivoxil, water-soluble high molecular weight substance and one or more pharmaceutically acceptable excipients is disclosed, wherein the weight ratio of high molecular weight substance to cefditoren pivoxil is greater than 1 :4, and a process for preparing the composition is also disclosed.
DE102009049505A1 Use of antimicrobial agent for preparing antiseptic for use in a disinfection method in which ultrasound is used simultaneously, where the disinfection method is e.g. wound healing, preoperative skin disinfection and surface disinfection Use of an antimicrobial agent for preparing an antiseptic for use in a disinfection method in which ultrasound is used simultaneously, is claimed. An independent claim is included for the antiseptic, for use in a disinfection method in which ultrasound is used simultaneously with the antiseptic, comprising one or more antimicrobial agent. - ACTIVITY : Antimicrobial; Vulnerary. - MECHANISM OF ACTION : None given.
US20050054696 Indole compounds and medicinal use thereof An indole compound represented by the formula (1) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof or a prodrug thereof is useful as a therapeutic agents for diabetes having an HLGPa inhibitory activity.
WO2009128383A1 3-PHENYLPYRAZOLO[5,1-b]THIAZOLE COMPOUND Disclosed is a compound represented by formula (I) or a salt thereof, which has an excellent antagonistic activity on a CRF receptor and also has sufficient levels of a pharmacological activity, safety and in vivo kinetics for use as a medicinal agent. [In the formula, R1 represents a group represented by formula -A11-A12; R2 represents a tetrahydrofurylmethyl group, a tetrahydropyranylmethyl group or a tetrahydropyranyl group; A11 represents a single bond, a methylene group or a 1,2-ethylene group; A12 represents a C1-6 alkyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkyl group having a methyl group; R3 represents a methoxy group, a cyano group, a cyclobutyloxymethyl group, a methoxymethyl group or an ethoxymethyl group; and R4 represents a methoxy group or a chlorine atom.]
CN101827596A Combination comprising purine derivatives and other compounds and the use thereof for the treatment of inflammatory and obstructive airway diseases A medicament comprising, separately or together: a component (A) which is an adenosine A2a receptor agonist as defined in the specification; and a component (B) which is one or more compounds selected from: (i) a corticosteroid, (ii) a beta-2 adrenoceptor agonist, (iii) an antimuscarinic agent, (iv) an A 2B antagonist, (v) an antihistamine, (vi) a caspase inhibitor, (vii) an ENaC inhibitor, (viii) an LTB4 antagonist, (ix) an LTD4 antagonist, (x) a serine protease inhibitor, (xi) a PDE4 inhibitor and (xii) a dual-acting beta-2 adrenoceptor agonist / muscarinic antagonist, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.
CN103070999A Medicine composition for treating premature ejaculation and preparation method of same The invention provides a medicine composition for treating premature ejaculation. The medicine composition comprises cuscuta chinensis, epimedium herb, cinnamon, manchurian wild ginger, fructus cnidii, gallnut, pomegranate bark, venenum bufonis, polygala tenuifolia, rhizoma acori graminei, musk and borneol. A preparation method comprises the following steps: taking the cuscuta chinensis, the epimedium herb, the fructus cnidii, the gallnut, the pomegranate bark, the polygala tenuifolia and the rhizoma acori graminei and putting these medicines into a medicine decocting container; adding water to the medicine decocting container to be 4 cm higher than the medicine surface; decocting the medicines for 30 minutes; filtering the decocted medicines; adding water to dregs to be 2 cm above the medicine surface; decocting the medicines for 20 minutes for future use; crushing the manchurian wild ginger and the cinnamon into a coarse powder; placing the coarse powder into the container; adding 100 parts of ethanol of 70 % by mass to the container for future use; taking a decocting solution and combining the decocting solution and an ethanol solution; uniformly stirring the mixed solution; standing the mixed solution for 24 hours; and filtering the mixed solution so as to obtain the medicine composition. The medicine composition provided by the invention has the advantages of obvious premature ejaculation curative effect and no side effect.
US8163743 4-carboxamide indazole derivatives useful as inhibitors of PI3-kinases The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.
WO2014020408A1 Compositions for a medical device comprising exopolysaccharide-producing bacterial strains in association with gums and/or gelatines The present invention relates to a composition for a medical device comprising a specific mucoadherent gelling complex composed of EPS, exopolysaccharides of bacterial origin produced in situ in the gastrointestinal tract by specific selected bacterial strains, in association with vegetable gums and/or animal and/or vegetable gelatines. Said complex is capable of establishing a complete barrier effect of a mechanical type extending throughout the whole gastrointestinal tract and can be used as a medication for the prevention and treatment of all pathologies connected to a deficiency in the barrier effect in the gastrointestinal area due to a low production of mucus, such as, by way of non-exhaustive example, intestinal permeability and bacterial translocation.
EP1214295B1 Hydroxyacetamidobenzenesulphonamide derivatives A compound of formula (I) wherein: R?1, R2, R3, R4, R5, R6 and R7¿ are as defined within; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
CN103145779A 3,5-dimethyl-8-(3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-oxo) heterochromatic original alkyl-1-one, preparation method and application thereof The invention discloses a compound with a structural formula as shown in the specification, and further provides a method of preparing the compound by fermenting and culturing a bacterial strain CGMCC No. 5410 of Xylarid sp. The compound has good antineoplastic activities for human non-small-cell lung cancer cells, human breast cancer cells, human pancreas cancer cells and many other tumor cells, and can be used for preparation of antitumor drugs.
WO2005027970A1 Drugs for treating cancer It is intended to provide a drug for treating cancer wherein a therapeutic effect on cancer is synergistically enhanced by using a substance inhibiting the activities of insulin-like growth factor-I (IGF-I) and insulin-like growth factor-II (IGF-II). Namely, a drug for treating cancer, which comprises a substance inhibiting the activities of IGF-I and IGF-II, to be administered together with exposure to radiation; and a drug for treating cancer comprising a substance inhibiting the activities of IGF-I and IGF-II combined with a substance having an antitumor activity.
US20080227821 N-substituted tricyclic 3-aminopyrazoles as anti-mitotic tubulin polymerization inhibitors The invention is directed to compounds having the following structures: N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine; 3-[3-(3-Bromo-phenylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol; or 3-[3-(2-Chloro-pyridin-4-ylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol, and N-oxides, pharmaceutically acceptable salts, solvates, tautomers and stereochemical isomers thereof and the uses of such compounds as inhibitors of tubulin polymerization and for the treatment of solid tumors. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
CN102018689A New application of curcumin The invention discloses application of curcumin to preparation of medicaments for preventing and/or treating autosomal dominant polycystic kidney disease. A madin-darby canine kidney (MDCK) vesicle model is used for screening to obtain the curcumin which inhibits formation and growth of vesicles. An experimental result shows that: the curcumin has an obvious inhibiting effect on the formation and growth of MDCK vesicles and the effect of the curcumin is in dose response relationship; the curcumin has no cytotoxicity to MDCK cells, so that the vesicle inhibiting effect of the curcumin is independent of the cytotoxicity; the curcumin does not obviously induce MDCK cell apoptosis, so that the vesicle inhibiting effect of the curcumin is independent of cell apoptosis promotion of the curcumin; the curcumin can promote the MDCK cells or vesicles to form tubular structures; and the effect is in dose response relationship; and the curcumin has an inhibiting effect on the growth of the embryonic kidney vesicles. The curcumin is expected to be developed into a specific medicament for preventing and/or treating autosomal dominant polycystic kidney disease.
US20100324068 Chemical compounds 785 DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X2 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or —CONHSO2Me or —CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is —CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.
WO2008003245A1 The use of rosmarinic acid in the manufacture of medicaments for treating or preventing hepatic and renal diseases The present invention has determined that rosmarinic acid could treat or prevent hepatic fibrosis and renal fibrosis by inhibiting the expression of connective tissue growth factor in many tests. The new use of rosmarinic acid in the manufacture of medicaments for preventing and treating chronic hepatitis, chronic renal failure and diabetic nephropathy is provided based on the fact.
WO2014155376A1 Methods of treating myeloid leukemia There is provided a method of treating a myeloid leukemia. The method includes the step of administering to a subject in need thereof a therapeutically effective amount of a CXCR4-antagonistic peptide and a therapeutically effective amount of a chemotherapeutic agent.
EP2698368A1 Novel pyrazole derivative Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.
CN103301128A Esomeprazole sodium composition for injection The invention provides an esomeprazole sodium composition for injection, relating to the field of drugs and drug production technology. The main drug of the composition includes esomeprazole sodium and melatonin, wherein the melatonin comprises a quick release part and a cyclodextrin-inclusion slow release part. The esomeprazole sodium composition for injection is fast in potency and reliable in effect, and applicable to a patient who is not suitable for orally taking medicine, and a drug which is not suitably taken orally; the drug administration design of combining quick release and slow release meets the physiological secretion characteristic of the melatonin, solves the defect of short half life period of the melatonin, and improves the bioavailability of the product; the synergism of the esomeprazole sodium on treating reflux esophagitis can be achieved, gastric dynamics can be enhanced to promote gastric emptying. The coordinated movement of stomach antrum, pylorus and duodenum can be promoted, and the reflux of gastric content can be completely prevented.
CN102093187A Polyketone compounds and application thereof The invention relates to polyketone compounds extracted from fermentation liquor of marine sourced microorganisms and application thereof, in particular to two polyketone compounds separated from the fermentation liquor of a fungus Nigrosporasphaerica of Xylocarpus Granatum which is a mangrove plant collected from the intertidal zone of the South China Sea and application thereof, and more particularly relates to novel polyketone compounds with certain cytotoxin activities and immunologic adjuvant functions. The structural formulas of the polyketone compounds are shown as the graph 1 and the graph 2 in the specification. In the invention, the activities of the novel compounds are tested by using in vitro cytotoxin experiments, and the result indicates that the two compounds represent different degrees of activities to tumor cells; and in addition, the immunoregulatory activities of the compounds are also primarily tested by utilizing immune regulation experiments of concanavalin stimulation, and the testing result indicates that the compounds have certain immunologic adjuvant functions, but the specific mechanisms are not definitely reported.
US20050059712 Immunosuppressants for treating skin disorders, acne, alopecia, estrogen- or androgen-dependent tumors, rheumatoid arthritis, type I and II diabetes, lupus erythematosus, multiple sclerosis, ulcerative colitis, Crohn's disease, psoriasis, contact dermatitis, graft versus host disease, eczema, asthma A compound of formula wherein R1 is haloalkyl, alkenyl, phenyl, thienyl, pyridine, benzthiazolyl, chromanyl (1,2-dihydrobenzopyranyl) or (C6-18)aryl, and R1 or R2 independently of each other are substituted (C4-8)cycloalkyl, a substituted bridged cycloalkyl system, substituted piperidine, substituted tetrahydropyridine, or a substituted bridged heterocyclic system, useful as a pharmaceutical.
EP2590645A2 Methods for treating bipolar disorder The invention is directed to a method of treating bipolar disorder in a subject, comprising administering a therapeutically effective amount of a carbamate compound, or pharmaceutically acceptable salt or amide thereof.
US20120219510 Natural extract from whole banana fruit (musa spp) A natural Extract from whole Fruit of Banana (Musa Spp.), (including edible portion and peel), whether unripe or ripe, containing mainly natural Melatonin, Serotonin, Catecholamines and its precursors; amino acids tryptophan and tyrosine; minerals potassium, magnesium, phosphorous and antioxidants. The extract contains very minimal or no carbohydrates.
WO2010103312A1 Hydroxymorpholiness and their use for the treatment of inflammatory disorders and pain A compound useful for therapy of a pain or inflammatory condition, is of formula (I): wherein: R1 is aryl or heteroaryl and is optionally substituted with one or more groups selected from alkyl, CF3, OR6, OCOR6, CONH2, CN, Cl, Br, I, N(R6)2,NO2, NHCHO, NHCONH2, NHSO2R6, CON(R6)2, S(O)nR6, CH2OH and OCON(R6)2 wherein n is 0-2; R2 and R3 are each H, alkyl, cycloalkyl or CH2 OH, or CR2R3 forms a ring; R4 is H or alkyl; and R6 is H, alkyl or cycloalkyl; or a salt thereof.
EP1121114B1 Use of gaba analogs for the manufacture of a medicament for the treatment of mania and bipolar disorders The present invention is a novel therapeutic use of pregabalin, its derivatives, and the pharmaceutical salts thereof. The compounds are useful in the treatment of mania in all its various forms whether acute or chronic, single or recurrent, and whether or not it is associated with depression. The invention further includes the preventive treatment of bipolar disorder.
US7323164 Can be administered in conjunction with radiation or chemotherapeutic agents. The present invention relates to the anti-cancer activity of IL-24 polypeptide molecules. IL-24 is a cytokine involved in inflammatory processes and human disease. The present invention includes Use of IL-24 for decreasing proliferation of ovarian cancer cells, treating ovarian cancer, amongst other uses disclosed. IL-24 polypeptides can be administered alone, or can be fused to cytotoxic moieties, and can be administered in conjunction with radiation or chemotherapeutic agents.
WO2012098068A1 Pyrazolo pyrimidines as dyrk1a and dyrk1b inhibitors Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
US20110207810 N1-benzo[1,3]dioxol-5-ylmethyl-n2-substituted biguanide derivative, preparation method thereof, and pharmaceutical composition containing same The present invention provides an N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.
EP1720854A1 Phthalzinone derivatives as pde4 inhibitors The compounds of a certain formula (1), in which R1, R2, R3, R9 and n have the meanings as given in the description, are novel effective PDE4 inhibitors.
US20080176848 e.g. N-Hydroxy-3-{1-[4-(1-methyl-1H-indol-5-yl)-benzenesulfonyl]-1H-pyrrol-3-yl}-acrylamide; antiproliferative, anticarcinogenic, antiinflammatory, neuroleptic agent, autoimmune disorders Compounds of a certain formula (I) in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.
US20100120857 Use of tris-quaternary ammonium salts as pain modulating agents Provided are tris-quaternary ammonium compounds which are modulators of nociception and pain.
US20080275003 Phospholipase inhibitor; prevention or therapy of microbial infection; bactericides; fungicides; viricides; parasiticides; using quaternary or phosphonium group containing compounds The present invention relates to bis-cationic compounds comprising quaternary ammonium groups and/or quaternary phosphonium groups. The invention also relates to the use of bis-cationic compounds as Phospholipase B inhibitors and the use of bis cationic compounds for the treatment or prevention of microbial infection.
WO2006040151A8 Subsituted hydroxyethylamine compounds for treating alzheimer’s disease The present invention relates to novel hydroxyethylamine compounds of formula (1) wherein, inter alia, A-B represents -NR5-SO2-;-W-represents -(CH2)3- or -C(H)=C(H)-CH2-; X-Y-Z represents -C=CR8 -NR9-, having Asp2 (β-secretase, BACE1 or Memapsin-2) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β- amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
US20100286251 Mammalian Genes Involved In Viral Infection And Tumor Suppression The present invention provides methods of identifying cellular genes used for viral, bacterial or parasitic growth. Also provided by the present invention are nucleic acids related to and methods of reducing or preventing viral, bacterial or parasitic infection.
CA2314775C Novel lactic acid bacterial preparation that reduces triglycerides and cholesterol Although the inventors previously found that the novel species designated Lactobacillus clearans was highly effective for health purposes, they noted in particular that this species lacked sufficient intestinal purification action. Efforts to produce a species of higher potency and the like to remedy this drawback led to the unavoidable conclusion that the use of a bacterium by itself produced limited results. The concurrent use of another active substance was thus considered in seeking a lactic acid bacteria preparation capable of invigorating healthy individuals, and of renewing a sense of well being and restored health in semi-sick individuals or semi-healthy individuals. The invention relates to a lactic acid bacteria preparation, comprising viable cells of Lactobacillus clearans, and either or both of viable and killed cells of Enterococcus faecalis capable of reducing one or more of at least triglycerides and cholesterol.
US20090010927 Mapkap kinase-2 as a specific target for blocking proliferation of P53-defective cells The present invention relates to compounds and pharmaceutical compositions for treating cellular proliferative disorders, e.g., in patients having one or more p53-deficient cells, screening assays for identifying such compounds, and methods for treating such disorders.
EP2002836A1 Cyclocondensed azaindoles active as kinase inhibitors Substituted cyclocondensed azaindole compounds of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.
CA2449312C Methods for the treatment of nail fungus and other microbial and mycotic conditions and compositions useful therefor In accordance with the present invention, there are provided methods for treatment of pathological conditions of the nail, said method comprising topically applying to the affected area an effective amount of a composition comprising an optionally substituted lower alcohol and an optionally substituted lower carboxylic acid. Invention methods effectively treat bacterial or fungal infections of the nail by utilizing a low viscosity composition having the ability to penetrate through and underneath the nail plate, thereby attacking the infection at its source.
WO2010137351A1 Aryl substituted carboxamide derivatives as calcium or sodium channel blockers The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.
CN101036645A Pharmaceutical composition for treatment of acne The invention provides matrine and/or oxymatrine and use of angelica oil for treating acne, wherein, the matrine and/or oxymatrine and the angelica oil can be used independently, or used by combined to recipes. Preparations for oral taking such as soft capsule, capsule, troche, etc. or preparations for external application such as ointment, emulsion, etc. are produced by a manner of pharmacy. In addition, injection, e.g., injecta and the like is prepared, thus the invention can perform administration by injecting, oral taking or external application.
EP1793842A2 Treatment for cancer-related fatigue The present invention is concerned with the treatment of cancer patients suffering from severe and persistent fatigue, diagnosed as Cancer-Related Fatigue (CRF), with thyrotropin-releasing hormone (TRH) and analogs of TRH. A method for the treatment of CRF and the use of TRH and analogs of TRH in the manufacture of a medicament for the treatment of CRF is provided.
WO2011156970A1 Uses of mtea in diagnosis and treatment of malignant tumor The invention discloses a multiple tumor expressed antigen (MTEA) which can be used as a marker of malignant tumors, and the uses thereof for diagnosis and treatment of malignant tumors such as liver cancer. The invention also discloses a kit for diagnosis of malignant tumors, a pharmaceutical composition for treatment of malignant tumors, and a method for preparing the inclusion body antigen of MTEA protein.
US20120207856 MSH3 Expression Status Determines the Responsiveness of Cancer Cells to the Chemotherapeutic Treatment with PARP Inhibitors and Platinum Drugs Methods for treating a patient at risk for or diagnosed with colorectal cancer are disclosed herein. The method of the present invention determines the overall expression of MSH3 in cells suspected of being colorectal cancer cells from the patient and predicting the efficacy of therapy with a genotoxic anti-neoplastic agent for treating the patient, wherein a decrease in the overall expression of MSH3 in the patient cells when compared to the expression of MSH3 in normal colorectal cells indicates a predisposition to responsiveness to genotoxic anti-neoplastic agent therapy, wherein the therapy comprises administering an effective amount of the genotoxic anti-neoplastic agent therapy to patients.
EP1517691A1 Use of dopamine receptor agonists for the treatment of cutaneous tumors, warts, and scars The invention relates to the use of dopamine receptor agonists, particularly dopamine D2 receptor agonists such as bromocriptine, for the local treatment of cutaneous tumors, warts, and scars, preferably in combination with dimethyl sulfoxide.
US20140079828 Methods for increasing human growth hormone levels Embodiments of the invention generally relate to methods and supplements for increasing human growth hormone (hGH) levels in healthy human beings.
WO2007115973A3 Food products for hypophosphoric normo-, hyper- and hypoproteic diets, and their use for nutrition of subjects in need of a low phosphorus level diet The present invention relates to an alimentary component comprising a physiologically acceptable phosphorus binding agent, in particular polyallylamine hydrochloride, polyallylamine carbonate, lanthanum carbonate, aluminium hydroxide, magnesium acetate, magnesium carbonate, calcium carbonate, calcium acetate, calcium citrate, calcium alginate, styrene divinylbenzene ionic exchange resin, stabilized polynuclear iron hydroxide, calcium acetate plus magnesium carbonate and chitosan. Said component is useful in the nutrition of subjects in need of a low phosphorus level diet.
WO2008150231A1 New heterocyclic compounds for treatment of respiratory, airway or inflammatory disorders The present invention relates to new compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein Q, X, Y, A, R1, R2, R3, R4, R5, R6 and m, n, and p are defined as in claim 1, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions comprising said compounds and to the use of said compounds in therapy.
WO2006086837A1 Non-surgical mulesing A non-surgical method for the removal from an animal of skin at selected locations, said method comprising administration to the skin of such locations an effective amount of a sclerosing agent such as an anionic surfactant capable of causing skin necrosis.
CA2566180A1 Use of targeted oxidative therapeutic formulation in treatment of cancer A pharmaceutical formulation and its use. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, Su has ozone; a penetrating solvent, such as dimethylsulfoxide (~DMSO~); a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone. The pharmaceutical formulation is used to effectively treat patients affected with cancer, such as lymphoma.
US20120021013 Composition Containing Sulfoalkyl Ether Cyclodextrin and Latanoprost An aqueous composition of latanoprost and SAE-CD is provided. The composition possesses improved stability over otherwise similar compositions excluding SAE-CD. Methods of and systems for treating diseases, disorders, conditions or symptoms of the eye that are therapeutically responsive to latanoprost are also provided.
CN101061861A Health-care hypoglycermic food and its preparing method The invention relates to an auxiliary antihypelipidemic health food and process for preparation, wherein the food comprises the following constituents (by weight portions): glucosamine 20-40, ginkgo leaf extract 1-20, balsam pear fines 10-30, pumpkin powder 15-50, sweetener 1-10. The preparing process consists of proportioning, mixing and packaging.
CN101380315A Diphenhydramine filling capsule The invention provides a capsule which has favorable adaptability at administration, is difficult to cause softening and/or cracking of a surface membrane of the capsule, and is filled with solution containing diphenhydramine or salt thereof. The capsule is characterized in that the solution containing the diphenhydramine or the salt thereof is filled in the surface membrane of the capsule containing polyethylene glycol and gelatin.
US20090252721 Differentially expressed tumour-specific polypeptides for use in the diagnosis and treatment of cancer The invention relates to agents and methods for the diagnosis, prognosis and treatment of cancer. Specifically, the invention relates to the use of nucleic and amino acid sequences encoding transmembrane superfamily member 6 (TM4SF6), synaptophysin like protein (SYPL), stomatin like 2 (STOML2), Ras related GTP binding protein RAGA), nucleotide sensitive chloride channel 1A (CLNS1A), prion protein (p27-30) (PRNP), guanine nucleotide binding protein beta 2-like 1 (GNB2L1), guanine nucleotide binding protein 4 (GNG4), integral membrane protein 2B (ITM2B), integral membrane protein 1 (ITM1), transmembrane 9 superfamily member 2 (TM9SF2), opiate receptor-like 1 protein (OPRL1), low density lipoprotein receptor-related protein 4 (LRP4), human glomerular epithelial protein 1 (GLEPP1), toll-like receptor 3 (TLR3), and/or zona pellucida glycoprotein 3A (ZP3) for the diagnosis of both early and late stage non-steroid specific cancers, cancer prognosis, as well as screening for therapeutic agents that regulate the gene expression and/or biological activity of said proteins. This invention further relates to the biological technologies designed to inhibit the gene expression and/or biological activity of said proteins including using agents identified in screening assays described herein, vector delivery of antisense polynucleotide sequences, and antibody targeting of said proteins. In specific embodiments, the proteins are of human origin.
US20090170788 Novel use of 1, 2, 3, 4, 6-penta-o-galloyl-beta-d-glucose The present invention relates to novel use of 1,2,3,4,6-penta-O-galloyl-beta-D-glucose. More particularly, the present invention relates to a pharmaceutical composition and cosmetic composition for preventing and treating skin disease, comprising 1,2,3,4,6-penta-O-galloyl-beta-D-glucose represented by formula 1 as an active ingredient. Also, the invention relates to a method for preventing and treating skin disease using 1,2,3,4,6-penta-O-galloyl-beta-D-glucose, and to the use of 1,2,3,4,6-penta-O-galloyl-beta-D-glucose.
WO2010123047A1 Crystal of benzoxazinone compound Disclosed is a crystal of 2-hexadecyloxy-6-methyl-4H-3,1-benzoxazin-4-one useful as a preventive or therapeutic agent for obesity and the like. Specifically disclosed is a crystal of 2-hexadecyloxy-6-methyl-4H-3,1-benzoxazin-4-one having a powder X-ray diffraction pattern in which characteristic peaks appear at powder X-ray diffraction interplanar spacings (d) of around 16.54 ± 0.2, 13.26 ± 0.2, 4.70 ± 0.2, 4.38 ± 0.2, and 3.67 ± 0.2 Ǻ.
EP1848422A2 Method for decreasing cartilage damage in dogs A method for modulating enzymatic degradation of articular cartilage in a dog comprises administering to the dog an enzymatic degradation modulating effective amount of eicosapentaenoic acid (EPA), for example as a component of a food composition. By practice of the method in a dog having arthritis, mobility of the dog can be increased, weight bearing in an arthritic limb can be increased, and/or pain associated with arthritis can be reduced.
US20090111890 to stimulate hair growth, restore hair color to depigmented hair, alopecia; side effects reduction; (16-(3-chlorophenoxy)-17, 18, 19, 20-tetranor PGF2 alpha ) cyclopropyl methyl amide The present invention relates to the formulation and delivery of prostaglandin analogs to treat epithelial-related condition. In some embodiments, the compositions of the invention are used to stimulate hair growth. In some embodiments, the compositions of the invention are used to restore hair color to depigmented hair.
CN101415464A Solid oral compositions based on s-adenosyl methionine and/or NADH and process for obtaining them This invention relates to solid oral compositions based on SAMe and/or NADH or their salts in association with calcium oxide and/or calcium hydroxide and a process for obtaining them. This invention also relates to a method for stabilising a solid oral composition based on SAMe and/or NADH or their salts, making use of calcium oxide, calcium hydroxide optionally in association with malic acid, glutamic acid, xylitol, calcium sulphate hemihydrate, magnesium oxide and/or mixtures thereof. This invention also relates to the use of SAMe or its salts in association with calcium oxide and/or calcium hydroxide with the possible further addition of melatonin and/or l-theanine and/or 1-tryptophan and/or 5-hydroxytryptophan for the treatment of depressive states.
CN102153558A Derivative of multi-target antitumor inhibitor 2-aminopyrrole-triazine and synthesis method thereof The invention discloses a derivative of a multi-target antitumor inhibitor, namely 2-aminopyrrole-triazine and a synthesis method thereof, and relates to the technical field of the treatment of abnormal cells in mammals. The derivative is synthesized by taking ethyl isocyanoacetate as a starting point through a chemical synthesis method, and has the advantages of mature process, short production period, environment friendliness, low cost and the like. The product can be used as a heat shock protein (Hsp) 90 multi-target antitumor inhibitor, can inhibit Hsp90, and promote the degradation of Hsp90 effect proteins which play an important role in tumor growth signal pathways through ubiquitination, so that multiple targets of the tumor growth signal pathways are blocked and the growth of tumor is effectively prevented. The derivative has higher affinity with tumor cells, can selectively kill the tumor cells, and promote the degradation of primer proteins thereof through ubiquitin-proteasome pathways, so that the effects of tumor treatment and resistance of the targets are achieved, and the derivative has strong action and small side effect.
US20090318553 Use Of Docosahexaenoic Glycerides For The Treatment Of Tumorous Diseases The present invention relates to the use of an oil enriched in docosahexaenoic acid, which is conjugated to triglyceride, for manufacturing a pharmaceutical composition for the treatment of a tumorous disease, said oil being enriched in a concentration of up to 70% by weight in relation to the total weight of said pharmaceutical composition, and said docosahexaenoic acid being in a percentage of at least 50% in relation to the total fatty acids in said oil.
CN101530619B Method for preparing water soluble pegylation hydroxycamptothecine derivatives The invention provides a method for preparing water soluble pegylation hydroxycamptothecine derivatives by solid phosgene, which belongs to the technical field of water soluble polymer synthesis and degradable medical application. The method adopts BTC is adopted as a coupling agent, selects methenyl chloride as a solvent and pyridine as a catalyst, uses the characteristic of bifunctionality of hydroxycamptothecine, and introduces water soluble polyethylene glycol into the 10th position and the 20th position of the hydroxycamptothecine through a carbonic ester bond. A yellow solid product canbe obtained by precipitating and drying by a mixed solution of absolute methanol and absolute aether. The polymer is connected by ester bonds, can be degraded in body via metabolism, can effectively avoid the problem of kidney accumulation generation, and can prominently improve water solubility, structure stability, and the like of the hydroxycamptothecine.
CN103360298A Preparation method of beta type silodosin crystal The invention discloses a preparation method of a beta type silodosin crystal. Silodosin is a medicament which is clinically used for treating benign prostatic hyperplasia, and three crystal forms, namely alpha, beta and gamma exist. Although the beta crystal form silodosin can be used as an active ingredient of an oral medicament, the preparation method in the prior art has the shortcomings of more process steps, low yield, low purity and the like. According to the preparation method disclosed by the invention, the beta crystal form silodosin is obtained by selecting an appropriate halogenated alkane type solvent and adopting a mild crystallization way. The method has the advantages of stable process, simplicity in operation, convenience, quickness, higher yield and higher purity, the used solvent is very easy to remove, and the method can be used for industrial production.
WO2010111468A2 RNA INTERFERENCE MEDIATED INHIBITION OF THE NERVE GROWTH FACTOR BETA CHAIN (NGFß) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (SINA) The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of NGFβ gene expression and/or activity, and/or modulate a NGFβ gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against NGFβ gene expression.
WO2010088368A2 Imidazopyrazines as protein kinase inhibitors In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.
CN102125577A New azithromycin ophthalmic preparation composition and preparation method thereof The invention relates to a new azithromycin ophthalmic preparation composition and a preparation method thereof, belonging to the field of pharmaceutical preparation. The invention adopts a liposome technology and an in situ gel technology to dissolve the main medical component azithromycin in a bilayer lipid membrane, thus improving the stability of the preparation and relieving irritation on eyes; simultaneously the release of the azithromycin is controlled, thus improving the bioavailability of the main medicine; the administration frequency is reduced, thus improving the compliance of patients; and the azithromycin ophthalmic preparation composition is easy to fill, thus facilitating industrialized production.
CN1785197A Method for preparing colon locatization controlled-release tablets contg. Azulfidine A process for preparing the release-controllable locating-in-colon tablet of sulphasalazine for treating colitis is disclosed.
CN1931150A Elemene soft capsule and its prepn process The present invention is elemene soft capsule as one kind of antitumor medicine and its preparation process. The elemene soft capsule consists of capsule covering and inclusion. The inclusion includes elemene, vegetable oil and surfactant; and the capsule covering is made with adhesive, plasticizer, opacifier and water in the weight ratio of 1 to 0.3-0.45 to 0-1 to 0.7-1.4, and has pH value controlled in 5.0-7.0. The elemene soft capsule has the bad smell of elemene masked, and has high stability.
CN103611075A Bezoar refreshing preparation and preparation method thereof The invention discloses a bezoar refreshing preparation which is characterized by being prepared from the following components in parts by weight: 180-220 parts of buffalo horn concentrate powder, 80-120 parts of bezoar, 80-120 parts of hawksbill, 80-120 parts of radix curcumae, 80-120 parts of jasmine, 80-120 parts of scutellaria baicalensis, 80-120 parts of coptis chinensis, 80-120 parts of cinnabar, 80-120 parts of realgar, 45-55 parts of pearls, 22-28 parts of borneol and 4-6 parts of musk. The bezoar refreshing preparation disclosed by the invention is used as a medicine by whole powder, and is not extracted, so that no loss of medicinal components exists. The bezoar refreshing preparation has the functions of mainly clearing away heat and toxic materials, relieving convulsion and inducing resuscitation, and is used for symptoms such as hyperpyrexia of fever, coma and convulsions, dysphoria, pediatric epilepsy and insomnia. The preparation mainly has the effects of exciting the central nervous system, preventing bacteria and inflammation, sedating, preventing convulsions and the like.
US20100179120 Novel amide derivative for inhibiting the growth of cancer cells The present invention provides a novel amide derivative and a pharmaceutically acceptable salt thereof which selectively and effectively inhibits the growth of cancer cells induced by the overexpression of an epidermal growth factor receptor and also prevents the development of drug resistance caused by the mutation of EGFR tyrosine kinase, and a pharmaceutical composition comprising same as an active ingredient.
CN1723901A Fleroxacin lactate dispersion tablet, and its prepn. method A dispersing tablet of florocixine acetate is proportionally prepared from lactose, carboxymethyl starch sodium, cross-linked carboxylmethyl cellulose sodium, cross-linked polyvidone, magnesium stearate, SiO2 and PVPK30 solution. Its preparing process is also disclosed.
WO2007091946A1 Use of spiro [ imidazolidine-4, 3'-indole] 2, 2', 5' (1h) triones for treatment of conditions associated with vanilloid receptor 1 The present invention relates to a new use of spiro-hydantoin derivatives of formula (I), or salts, solvates or solvated salts thereof, as well as to new compounds, a process for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.
US20130172970 Heat Patch For Obesity Provided in the present invention are a composition for ameliorating or treating obesity and methods of making and using the same.
CN1640409A High-purity scutellarin injection agent The present invention relates to a high-purity breviscapine injection. Said injection contains breviscapine whose purity is 90.0%-99.5% (containing end point) and physiologically-acceptable salt.
US20090012026 Association Between the Tdoa Gene and Osteoarthritis The present invention arises from the identification of an association between the TDOA gene and osteoarthritis (OA). It therefore relates to diagnostic techniques for determining a patient's susceptibility to develop OA by detecting all or part of the TDOA gene, its precursors or products (mRNA, cDNA, genomic DNA, or protein). In particular, the invention relates to methods and materials for analysing allelic variation in the TDOA gene, and to the use of TDOA polymorphisms in the identification of an individuals' risk to develop OA. The TDOA protein has been found to bind to α-paxillin, a protein involved in integrin signal transduction which itself is a process with strong links to OA. The invention is thus also directed to methods for identifying modulators of OA, which modulate the TDOA gene or interfere with TDOA:α-paxillin binding.
CN1957923A A kind of controlled release injection of carried fluorouracil and synergis A slowly-release anticancer medicine in the form of injection or implant is disclosed. Said slowly-release injection is composed of a special solvent containing suspending aid and the slowly-release microballs consisting anticance medicine, iterstitial hydrolyte and slowly-releasing auxiliary. Said anticancer medicine is chosen from 5-FU, oxaliplatin, etc. Said interstitial hydrolyte is chosen from collagenase, relaxin, etc. Said slowly-releasing auxiliary is chosen from polylactic acid, FAD, polyethanediol, etc.
US7709461 Administering an aerosol of dry polysaccharide such as heparin of given particle size diameter The invention relates to methods for delivering polysaccharides by a pulmonary route to achieve local and systemic therapeutic effects. The polysaccharides may be formulated or unformulated and in some instances have an extremely fast absorption rate.
US20110028505 Compositions and methods for reducing food cravings Disclosed are compositions for reducing food cravings, comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound is an α-MSH agonist. Also disclosed are methods of reducing food cravings, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity.
CN1899291A External use antifungal compound composition and its use The present invention relates to antifungal composition with two or more active components and its application in medicine, cosmetics and sanitary articles. The externally applied antifungal composition butenafine, butenafine hydrochloride or ketoconazole in 0.1-10 wt%, and mometasone furoate in 0.001-10 wt%, except substrate. Animal test shows that the antifungal composition has obvious synergistic effect in resisting Trichophyton mentagrophytes infection.
EP1501515B1 Triaryl-oxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors The present invention relates to triaryl-oxy-aryloxy-pyrimidine-2,4.6-trione; metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, W. and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
CN103536529A Ceftiofur-containing long-acting injection and preparation method The invention relates to the application of sucrose acetate isobutyrate to the preparation of an oily injection for veterinary use, and specifically relates to preparation of a ceftiofur hydrochloride long-acting injection by using the combination of sucrose acetate isobutyrate and hydrogenated castor oil or an aluminum stearate, wherein a dispersion medium is one or more than one of isopropyl myristate, benzyl benzoate and ethyl oleate. The preparation is good in slow release effect, stable in characters, good in histocompatibility and easy to prepare.
WO2009043296A1 Gambogic glycoside derivatives and analogs, the preparation and the application thereof The invention discloses gambogic glycoside derivatives and analogs represented by formula I, the preparation and the application thereof, wherein the substituents R1-R12 are defined as in the description. The gambogic glycoside derivatives and analogs of the invention were synthesized from extracted and purified gambogic acid. The obtained gambogic glycoside derivatives and analogs have antitumor, antivirus, antibacterial and antifungal activities and can be used as antitumor, antivirus, immune, antibacterial and antifungal medicines. The gambogic glycoside derivatives and analogs of the invention can be used together with other known antitumor, antivirus, immune, antibacterial and antifungal medicines.
US20090041720 Heteroaryl substituted thiazoles The invention provides heteroaryl substituted thiazolo compounds of Formula I and II and pharmaceutically acceptable salts thereof. The variables A and R3 to R7 are defined herein. The invention also includes methods for preparing compounds and salts of Formula I and II. The present invention also includes pharmaceutical compositions containing heteroaryl substituted thiazolo compounds and methods for using heteroaryl substituted thiazolo compounds, including methods for using the compounds in the treatment of hepatitis C virus.
CN102920730A Application of agaricus blazei murill polysaccharide extracts in lipid-lowering drug preparation The invention relates to a pharmaceutical application of polysaccharide extracts obtained from agaricus blazei murill. The molecular weight of the polysaccharide extracts is between 500 thousand to 1500 thousand. The preparation method is extracted by ethanol with concentration of 95%, and then removing extracting solution, adding water into residues to immerse in a warm mode, in the period, extracting water extract ethanol precipitation by assisting of ultrasonic, removing albumen by sevag method for sediment and trypsin method, and then chromatographically separating by sephadex gel columns. The application of the agaricus blazei murill polysaccharide extracts in lipid-lowering drug preparation has obvious pharmacological activities, obvious hypolipidemic effects and effects of anti-tumor, increasing immunity and regulating blood sugar level.
EP2440294A1 Benzimidazole derivatives useful as trpm8 channel modulators Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows wherein R0, R1, R2, R3, R4 and a are defined herein. The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and condition modulated by the TRPM8 (transient receptor potential melastatin subfamily type 8) channel. The present invention also relates to processes for the preparation of benzimidazole derivatives and to their use in treating various diseases, syndromes, and disorders, including, those that cause inflammatory pain, neuropathic pain, cardiovascular diseases aggravated by cold, pulmonary diseases aggravated by cold,, and combinations thereof.
WO2012156537A3 Lysine demethylase inhibitors such as cyclylcylopropamine derivatives for use in the treatment of thrombosis and cardiovascular diseases The invention relates to methods and compositions for the treatment or prevention of thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event. In particular, the invention relates to an LSD inhibitor such as a 2-cyclylcyclopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event.
CA2413163C 3'-prodrugs of 2'-deoxy-.beta.-l-nucleosides The present invention relates to compounds, compositions and methods for the treatment of a host infected with a hepatitis B virus. Specifically, compounds and compositions of 3'-esters of 2'-deoxy-.beta.-L-nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents. Compounds and compositions of 3',5'-esters of 2'-deoxy-.szlig.-L-nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents, are also disclosed.
EP1781639A1 Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase This invention comprises the novel compounds of formula (I) wherein R1 , R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
CN103211783A Dextromethorphan hydrobromide film-controlled slow-release pellet capsule The invention relates to a dextromethorphan hydrobromide film-controlled slow-release pellet capsule. A slow-release film of the dextromethorphan hydrobromide film-controlled slow-release pellet utilizes Eurdragit RS 30D as a film-formation material. A pellet core of the dextromethorphan hydrobromide film-controlled slow-release pellet contains sodium carboxymethyl starch having high expansibility, and also contains pharmaceutically-acceptable common excipients for the slow-release pellet, wherein preferably, the excipients comprise microcrystalline cellulose and lactose, and the pellet core comprises 5 to 20wt% of sodium carboxymethyl starch. The slow-release film comprises Eurdragit RS 30D, triethyl citrate as a plasticizer, and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit RS 30D to triethyl citrate to talcum powder is 30: 1: 4 and coating weight gain is in a range of 16 to 35%. The dextromethorphan hydrobromide film-controlled slow-release pellet comprises the pellet core containing sodium carboxymethyl starch having high water expansibility and thus after absorbing water, the dextromethorphan hydrobromide film-controlled slow-release pellet obviously expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore diameter is increased; and permeability is improved and the permeability reduction caused by film aging is compensated. Therefore, in middle and later stages, the dextromethorphan hydrobromide film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept prior to expiration date.
WO2011088209A2 1-deoxy analogs of vitamin d-related compounds This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.
WO2014159999A1 Cdk9 kinase inhibitors Disclosed are compound of Formula (Ia), wherein R1A, R1, R2, R10, J, L, T, X, Y, and Z are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions, comprising one or more compounds of Formula (Ia).
CA2588994A1 Methods and compositions for the treatment of pulmonary hypertension of the newborn The present invention is directed to a novel methods and compositions for the therapeutic intervention in persistent pulmonary hypertension of the newborn (PPHN). More specifically, the specification describes methods and compositions for treating various types of PPHN using compositions comprising BH4. Combination therapies of BH4 and other therapeutic regimens are contemplated.
CN103755719A Physalin B crystal and extraction and preparation methods as well as application of physalin B crystal in preparing anti-inflammatory medicines The invention discloses a physalin B crystal which belongs to a monoclinic system, wherein the space group is P2(1); the lattice parameters (i)a(/i) is equal to 12.4996 (2), (i)b(/i) is equal to 14.35620(10), (i)c(/i) is equal to 14.75190(10) and (i)beta(/i) is equal to 99.8740(10) degrees; the volume of the crystal cell is 2607.97(5)3; the crystalline density is 1.382mg/m<3>; (i)Z(/i) is equal to 4; F(000) is equal to 1152; the final departure factors (i)R1(/i) is equal to 0.0407, and (i)wR2(/i) is equal to 0.1056. The invention further discloses an extraction method of the crystal. The extraction method comprises the following steps: 1) extracting a physalis plant material to remove a solvent to obtain an extract; 2) repeatedly dissolving soluble parts of the extract by petroleum ether, standing and filtering; 3) repeatedly dissolving the extract treated by petroleum ether by ethyl acetate, standing, filtering, combining the filtrate and removing the solvent to obtain a solid; and 4) dissolving the solid, mixing a sample by silica gel, passing through a column by a dry method, carrying out gradient elution, collecting an eluant, repeatedly carrying out column chromatography, and finally, removing the solvent from the eluant. The invention further discloses an application of the physalin B crystal in preparing anti-inflammatory medicines. The crystal obtained by the invention has higher anti-inflammatory activity.
CN102552238A New application of luteolin The invention discloses new application of luteolin, namely application of the luteolin to preparation of medicines for treating fatty liver. Animal experiments indicate that the luteolin can reduce the content of cholesterol and triglyceride in blood and the synthesis of the triglyceride in liver to block the source of lipid accumulation in the liver, so the luteolin is widely applied to preparing the medicines for treating the fatty liver, is high in practicability and has good economic benefit and social effect.
US20090088373 Use of compositions to enhance innate immune response The present invention discloses methods of using of compounds for the enhancement of the innate immune system of a patient. In particular, the active compounds of the present invention include at least one calcineurin inhibitor, mTOR inhibitor or non-immunosuppresive derivative, or a derivative, isomer, or pharmaceutically acceptable salt thereof; and optionally, at least one calciferol or LMW inhibitor, or a derivative, isomer, or pharmaceutically acceptable salt thereof. Pharmaceutical formulations comprising same are also disclosed.
US20100168065 Quinolinone derivatives as parp and tank inhibitors The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.
CN1899300A Medicinal composition using amino glucose hydrochloride and chondroitin sulfate as active components and its preparing method and use The present invention relates to a kind of medicinal composition with amino glucose hydrochloride and chondroitin sulfate as active components and its preparation process and use. The medicinal composition is prepared through mixing amino glucose hydrochloride and chondroitin sulfate as active components and pharmaceutically acceptable supplementary material. It may be used in treating osteoarthritis of different body parts, such as knee joint, hip joint, wrist, etc. It may be prepared into various kinds of preparation forms.
WO2014092346A1 Bitter taste masked pharmaceutical formulation comprising corticosteroid, antihistamine and stevia The present invention relates to a bitter taste masked pharmaceutical formulation comprising: (i) corticosteroid or a pharmaceutically acceptable salt thereof; (ii) an antihistamine selected from the group consisting of olopatadine, azelastine and a pharmaceutically acceptable salt thereof; and (iii) stevia. The pharmaceutical formulation according to the present invention effectively blocks bitter taste of the active ingredients, thereby having improved taste and patient compliance, and thus can be efficiently used in the treatment of allergic rhinitis.
US20080031964 Combination therapeutic compositions and method of use The present invention provides pharmaceutical compositions and methods for the treatment of diabetes mellitus using combination therapy. The compositions relate to a compound of Formula I selected from one or more of betaines, lipidic betaines, betaine lipids and an antidiabetic agent such as sulfonylureas, biguanides, glitazones, .alpha.-glucosidase inhibitors, potassium channel antagonists, aldose reductase inhibitors, glucagon antagonists, activators of RXR, insulin therapy or other anti-obesity agent. The methods include the administration of the combination of compound of Formula I with antidiabetic agent where the two components are delivered in a simultaneous manner, where the compound of Formula I is administered first, followed by the antidiabetic agent, as well as wherein the antidiabetic agent is delivered first followed by the compound of Formula I.
EP1289522B1 Medicaments for the adjuvant therapy of dementia comprising alpha lipoic acid The invention relates to the use of α-lipoic acid in reduced or oxidised form, or derivatives thereof which have an intact dithiolane structure in the form of enantiomers, or pharmaceutically acceptable salts, amides, esters, thioesters, ethers or metabolites for the adjuvant treatment of dementia.
WO2006109190A1 Tetracyclic monoamine reuptake inhibitors for treatment of cns diseases and disorders Novel tetracyclic dibenzo (e,h) azulene compounds of formula (I); their pharmacologically acceptable derivatives; pharmaceutical compositions containing them and their activity and use in the treatment of central nervous system (CNS) diseases and conditions in humans and animals.
CN103159644A Curcuminoid condensed aromatic amine Schiff base derivative, as well as preparation method and application thereof in preparation of antibacterial medicaments The invention relates to a curcuminoid condensed aromatic amine Schiff base derivative, as well as a preparation method and an application thereof in preparation of antibacterial medicaments, belonging to the technical field of synthesized curcuminoid condensed 3, 5-diaromatic amine Schiff base derivatives and applications thereof. According to the technical scheme, the preparation method comprises the following steps: dissolving substituted aromatic amine in anhydrous ethanol, adding a catalytic amount of formic acid and anhydrous aluminum trichloride, stirring, dropwise adding a curcuminoid analog ethanol solution prepared by the above reaction, and protecting with nitrogen; and refluxing and separating a reactant through a silica gel chromatographic method to get a target product. The curcuminoid condensed aromatic amine Schiff base derivative is used for preparing the antibacterial medicaments and used for resisting staphylococcus aureus and streptococcus. The curcuminoid condensed aromatic amine Schiff base derivative disclosed by the invention has an obvious inhibiting effect on the Staphylococcus aureus and the streptococcus; and compared with curcumin wich is a parent body, the curcuminoid condensed aromatic amine Schiff base derivative has the advantages that the antibacterial effect is better, the antibacterial effective time is longer, and the bioavailability and the antibacterial activity are improved.
CN101279977A Refining method of benemicin raw material and benemicin solution prepared from the benemicin raw material The invention provides a refining method to prepare the material for rifampicin and rifampicin solution prepared with the material. In the refining process of the material for rifampicin, the ratio of water and other solvent is properly controlled, and appropriate amount of antioxidant and ph regulator, etc., are added; the material is heated into reflux state in the solvent to reduce the impurity to a reasonable amount; then the heat source in the mixture is removed through active carbon; after that, the mixture is filtrated and crystallized, and the crystal is separated out and dried at low temperature. High-purity material for rifampicin can be obtained through single or repeated operations. The rifampicin solution is prepared by adding appropriate solvent, chemical inhibitor, ph regulator into the high-purity material for rifampicin. The rifampicin solution is of the capability of enduring the condition of 115 DEG C/30min(F0 is bigger than 8)for sterilization and can be stored for more than 12 months without change.
CN102885809A Application of Aphanamixoid A in medicament for treating pancreatic cancer The invention discloses application of Aphanamixoid A in preparation of a medicament for treating pancreatic cancer and belongs to the technical field of new application of medicaments. In-vitro methyl thiazolyl tetrazolium (MTT) anti-tumor activity evaluation shows that the Aphanamixoid A has a remarkable inhibiting effect on growth of human pancreatic cancer cell lines PANC-1 and BXPC-3. Therefore, the Aphanamixoid A can be used for preparing the pancreatic cancer resistant medicament, and has a good development and application prospect. The Aphanamixoid A in preparation of the medicament for treating the pancreatic cancer is disclosed for the first time, the skeleton type is a brand-new skeleton type, and the Aphanamixoid A has unexpected strong inhibiting activity on pancreatic cancer cells.
US20120022015 Method of treatment and supplement A method of treatment and associated nutritional combination is disclosed. The method of treatment includes providing a patient with a nutritional combination including appropriate amounts of riboflavin, pyridoxine hydrochloride, and cyanocobalamin. The combination may further include thiamine mononitrate and calcium pantothenate, and may be in the form of an oral supplement such as a capsule or tablet. Alternatively, the combination may be a fluid for intravenous intake, and may further include thiamine hydrochloride, D-panthenol, water, benzyl alcohol, and sodium chloride. The treatement and combination of ingredients works synergistically together and is particularly effective in enhancing nerve regeneration in a variety of patients.
CN103462966A Application of Incarviatone A in medicaments for treating colorectal cancer The invention discloses an application of Incarviatone A in preparation of medicaments for treating colorectal cancer, and belongs to the technical field of a new application of medicaments. In-vitro methyl thiazolyl tetrazolium (MTT) anti-tumor activity evaluation discovers that the Incarviatone A has a prominent inhibiting effect on growth of human colorectal cancer cell strains LOVE1, LoVo, SW620 and SW480. Therefore, the Incarviatone A can be used for preparing anti-colorectal cancer medicaments, and has a good development and application prospect. The application of the Incarviatone A in preparation of the medicaments for treating the colorectal cancer is made public for the first time, the skeleton type is completely novel, and the Incarviatone A has an unexpectedly strong human colorectal cancer cell inhibiting activity.
EP2763998A1 Tri-heterocyclic derivatives, preparation process and uses thereof The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
WO2014091318A1 Reduced dose pharmaceutical compositions of fenofibrate The present invention provides a reduced dose oral pharmaceutical composition comprising mixture of nanoparticulate fenofibrate and micronized fenofibrate and one or more pharmaceutically acceptable excipients.
CN101376653A Flavonol compound, and preparation and use thereof The invention provides a flavonol compound, and also relates to a preparation method thereof, a pharmaceutical composition comprising the same as the active component, and the application of the compound and the pharmaceutical composition on the preparation of antiphlogistic. The compound has remarkable anti-inflammatory effect, and can be expected to be antiphlogistic. The provided flavonol compound has a structure formula as above.
US20100105678 Novel anxiolytic compounds The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.
EP1757292A1 Method of treating ocd and tic disorders The invention relates to the use of a compound of formula (I): wherein Ar, n, X and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for treating obsessive compulsive disorder, chronic motor or vocal tic disorder in a mammal, including a human.
WO2009073517A2 Intravesical compositions with valrubicin for the treatment of bladder cancer Compositions and methods for the treatment of bladder cancer include intravesical dosage forms of a neoplastic agent and a permeation enhancer. The neoplastic agent may be valrubicin. Pharmaceutical compositions include intravesical dosage forms of a neoplastic agent complexed liposomes. Tight junction openers may be used for the effective delivery of the neoplastic agent.
CN103372055A Extraction process of total polyphenol as hypoglycemic active ingredient in cinnamon, total polyphenol composition and application thereof The invention belongs to the field of food and drug biotechnologies, and relates to an extraction process of total polyphenol as a hypoglycemic active ingredient in cinnamon, a total polyphenol composition and an application thereof. The extraction process comprises the following steps of: crushing raw cinnamon into 20 to 200 meshes; performing continuous counter-current leaching at 40 to 100 DEG C with water serving as a solvent to obtain a leaching solution; separating the leaching solution; adding ethanol; precipitating; recovering ethanol; drying to obtain a crude extract; adding water to dissolve the crude extract; performing polyamide column chromatographic purification to the crude extract aqueous solution; and then drying the purified material to obtain the total polyphenol. According to the extraction process, auxiliary materials are added to the total polyphenol extract of the cinnamon to form the total polyphenol composition of the hypoglycemic active ingredient in the cinnamon. The auxiliary materials are added to the total polyphenol extract of the cinnamon and are used for preparing health care products, foods or medicines for preventing and treating diabetes. The extraction process is scientific and reasonable, low in cost and suitable for mass production. The total polyphenol extract can be used for preparing the health care products, foods or medicines for preventing and treating 2-diabetes.
US20110223216 Nanoparticles and Porous Particles and Methods of Making the Same The subject matter disclosed herein relates to compositions and methods for engineering porous particles for aerosol formulations for pulmonary drug delivery. Certain embodiments disclosed herein further relate to methods for stabilizing suspension-based formulations in hydrofluoroalkane propellants with nanoparticles.
WO2011054185A1 Optical isomers of aralkyl piperazine derivative, preparation methods and uses thereof Preparation methods of optical isomers of compound of formula (B) and preparation methods of optical isomers of compound of formula (A) by using the said optical isomers of compound of formula (B) are disclosed, in which chiral camphor sulfonic acid acts as resolution reagent and the optical isomer mixtures or racemes of compound of formula (B) are chemically resoluted.. By using the optical isomers of the present compound of formula (B), the optical isomers of compound of formula (A) which are useful as antidepressants can be obtained with high yield and high purify.
US20070031882 Methods and compositions for treating AIDS and HIV-related disorders using 1414, 1481,1553, 34021, 1720, 1683, 1552, 1682, 1675, 12825, 9952, 5816, 10002, 1611, 1371, 14324, 126, 270, 312, 167, 326, 18926, 6747, 1793, 1784 or 2045 molecules The present invention relates to methods for the diagnosis and treatment of AIDS or an HIV-related disorder or disorders. Specifically, the present invention identifies the differential expression of 1414, 1481, 1553, 34021, 1720, 1683, 1552, 1682, 1675, 12825, 9952, 5816, 10002, 1611, 1371, 14324, 126, 270, 312, 167, 326, 18926, 6747, 1793, 1784 and 2045 genes in tissues relating to AIDS or an HIV-related disorder, relative to their expression in normal, or non-AIDS or HIV-related disease states, and/or in response to manipulations relevant to AIDS or an HIV-related disorder. The present invention describes methods for the diagnostic evaluation and prognosis of various HIV-related disorders, and for the identification of subjects exhibiting a predisposition to such conditions. The invention also provides methods for identifying a compound capable of modulating AIDS or an HIV-related disorder or disorders. The present invention also provides methods for the identification and therapeutic use of compounds as treatments of AIDS or an HIV-related disorder.
US20110245309 N-methylpurine dna glycosylase and polymerase beta as biomarkers for alkylator chemotherapy potentiation Described herein is the finding that polymerase β (Polβ) and N-methylpurine DNA glycosylase (MPG) can be used as biomarkers to evaluate the sensitivity of a subject to combination therapy that includes treatment with either temozolomide (TMZ) and methoxyamine, or TMZ and a poly(ADP-ribose) polymerase (PARP) inhibitor. Thus, provided herein is a method of determining if a subject will be sensitive to TMZ and methoxyamine, or TMZ and a PARP inhibitor by measuring expression of Polβ and MPG in a sample from the subject and comparing expression of Polβ and MPG in the sample to a control. A decrease in expression of Polβ and an increase in expression of MPG relative to the control indicates the subject is sensitive to TMZ and methoxyamine, or sensitive to TMZ and the PARP inhibitor.
US20110217361 Group of Nucleic Acid Fragments for Prevention of HIV Infection or AIDS and the Usage Thereof The invention provides a group of nucleic acid fragments, shown in the sequence listing, for prevention of HIV infection or AIDS and the usage thereof. In the invention, a series of RNA fragments, which are highly homogenous to all the published HIV gene sequences, were obtained by homology compare. The double-stranded RNA (dsRNA) derived from these fragments can effectively inhibit the expression of the HIV genes. The RNA transcribed by plasmid, also can suppress the expression of the HIV in the cell. After the adenovirus or associated virus which carry DNA corresponding above RNA infect the cell, the transcription dsRNA can inhibit the expression of the HIV genes.
CN101020637B Preparation process and application of resemary acid The present invention discloses preparation process and application of rosemary acid, and features that rosemary acid and its derivative and mixture may be prepared into preparation for antagonizing tumor of digestive tract and other tumor and synergizing and attenuating tumor treating chemotherapeutic medicine and radiotherapy. Medicine preparation of rosemary acid and its derivative and mixturemay be used directly in treating primary or secondary thrombocytopenic purpura and leucopenia and thrombocytopenia caused by chemotherapy or radiotherapy. The present invention also provides process of extracting high purity rosemary acid and its derivative and mixture from Sarcandra glabra as the plant material.
WO2008035604A1 Composition for amelioration of brain function Disclosed is a composition which can ameliorate the brain function effectively and is safe. Specifically disclosed are: a pharmaceutical composition or a food/beverage additive composition comprising a Bacopa monniera extract and a milk-derived sphingophospholipid; a pharmaceutical composition or a beverage/food additive composition comprising bacoside and a sphingophospholipid; and a food or beverage comprising the pharmaceutical composition or the food/beverage additive composition.
US20080132556 3-hydroxymethyl-4hydroxy-phenyl- derivatives for the treatment of respiratory diseases The present invention relates to the use of the compounds of general formula 1 wherein the groups R1, X and Y may have the meanings given in the claims and in the specification, for preparing a pharmaceutical composition for the treatment of COPD (chronic obstructive pulmonary disease), as well as new compounds of general formula 1 and processes for preparing them.
CN103417558A Anti-coxsackievirus compound The invention belongs to the bio-pharmaceutical field, and relates to medicines utilizing hapagoside as an active component and applications of the medicines in the medicine field. Pharmacological experiments prove that the hapagoside has good inhibiting activity for coxsackievirus B3, and that the hapagoside can be used for treating coxsackievirus infection-caused related diseases comprising viral myocarditis and arrhythmia caused by the viral myocarditis.
US20080261953 Compounds, Compositions and Methods of Inhibiting Alpha-Synuclein Toxicity Compounds and compositions are provided for treatment or amelioration of one or more symptoms of α-synuclein toxicity, α-synuclein mediated diseases or diseases in which α-synuclein fibrils are a symptom or cause of the disease. In one embodiment, the compounds for use in the compositions and methods are heteroaryl acylguanidines, heteroarylhydrazones, dihy-dropyridones, heteroaryl and aryl styryl ketones, and heteroarylpyrazoles.
US7772228 Administering a rifamycin microbiocides for treating infections caused by Mycobacterium tuberculosis, Mycobacterium avium complex, Chlamydia pneumoniae or Helicobacter pylori A method for treatment of bacterial infections with rifalazil administered once-weekly, or twice-weekly. A method for treatment of tuberculosis caused by Mycobacterium tuberculosis, infections caused by Mycobacterium avium complex, infections caused by Chlamydia pneumoniae and infections caused by Helicobacter pylori by administering to a patient suffering from the bacterial infection 1-100 mg of rifalazil once or twice a week. In this dose regimen, the treatment is fast, efficacious and eliminates undesirable secondary symptoms observed with daily doses of 1-50 mg of rifalazil.
CN103315955A Sarafloxacin hydrochloride sustain-released injection and preparation method thereof The invention relates to a sarafloxacin hydrochloride sustain-released injection and a preparation method thereof, belongs to a medicinal preparation field. The sarafloxacin hydrochloride sustain-released injection is composed of sarafloxacin hydrochloride, an emulsifier, a suspending agent, a stabilizing agent, an antioxidant, plant oil for injection, and injection water. The preparation method comprises the following steps of: heating sieved sarafloxacin hydrochloride raw material drug, the plant oil for injection, the emulsifier and the antioxidant in a constant temperature magnetic stirrer, to obtain a mixture A; heating the suspending agent, a water-soluble emulsifier, the stabilizing agent and the injection water in the constant temperature magnetic stirrer, to obtain a mixture B; continuously adding the mixture A into the mixture B, mixing and shearing to obtain colostrums; complementing margin of the colostrum with injection water, then homogenizing, loading, and disinfecting with cobalt 60 ray, to obtain the product. The sarafloxacin hydrochloride injection with obvious sustain-released effect on intramuscular injection of livestock and poultry, can reduce stress reaction, mitigates culture labor intensity, and raises economic benefits and social benefits for livestock and poultry culture.
CN101983630A Composition for treating salpingitis of birds and preparation method thereof The invention discloses a composition for treating salpingitis of birds and a preparation method thereof, aiming to provide a composition for treating the bird salpingitis, which has quick response, can address both the symptoms and root causes, reduces drug resistance rate of pathogenic bacteria and intensifies the curative effect, and a preparation method thereof. The composition consists of the following raw materials in percentage by weight: 5 to 15 percent of amoxicillin, 5 to 15 percent of metronidazole, 5 to 15 percent of aspirin, 5 percent of sodium carbonate, and the balance of anhydrous dextrose. In the composition, the amoxicillin and the metronidazole have excellent internal absorption effect and can enter the position of oviduct, can be combined to kill pathogenic bacteria causing the salpingitis of birds, and can avoid treatment failures caused by diagnosis errors; the aspirin has the functions of anti-inflammatory and diminish inflammation, can eliminate inflammation response, and improves the curing effect; and the sodium carbonate has the function of solubilizing the amoxicillin and the aspirin. Therefore, the composition can be drunk with water and is convenient to use.
CN103059297A Multifunctional degradable polyasparaginate modified polymer and preparation method thereof The invention discloses a multifunctional degradable polyasparaginate modified polymer, and further discloses a preparation method of the modified polymer and a method for preparing micelle and micelle loaded medicines by using the material. The modified polymer has functions of temperature sensation, pH sensation, fluorescent tracking and targeting. The polymer can be processed so as to rapidly form micelle nano particles and medicine loads; the loaded medicine is high in encapsulation efficiency, and no toxic solvents are used. The main chain part of the polymer is biologically degradable polyasparaginate with low toxicity; a side group hydrophobic section component can be hydrolyzed by using a carbonic ester bond so as to lose hydrophobic groups convert into hydrophily; and a tumor targeting group can lead the medicine loading micelle to enter tumor cells in a targeting mode to degrade and release loaded toxic medicines, so that damage of chemotherapeutic medicines to normal human body tissue cells is avoided.
CN103356716A Fermented composition of multiple probiotics and composite medicinal and edible fungi, and preparation method and application thereof The invention discloses a fermented composition of multiple probiotics and composite medicinal and edible fungi, and a preparation method and an application thereof. According to the invention, a composite polysaccharide extract is obtained by enzymolysis and extraction of various medicinal and edible fungi by using compound enzymes, and the extract is subjected to symbiotic fermentation by using multiple intestinal probiotics, such that a fermented composition is obtained. The invention also relates to an application of the fermented composition in preparing health-care products used for preventing and treating tumors. The medicinal and edible fungi adopted by the invention are any three or more than three selected from lucid ganoderma, agaricus blazei murill, shiitake, and flammulina velutipes. The fungi are subjected to crushing, soaking, and enzymolysis; and bifidobacterium and lactobacillus are added for fermentation. Through symbiotic fermentation with the intestinal probiotics, the molecular weight of medicinal and edible fungi composite polysaccharide is substantially reduced, tumor cell inhibiting activity is substantially improved, and inhibition effect is substantially improved.
US20090263402 Growth Differentiation Factor-11 A transgenic non-human animal of the species selected from the group consisting of avian, bovine, ovine and porcine having a transgene which results in disrupting the production of and/or activity of growth differentiation factor-11 (GDF-11) chromosomally integrated into the germ cells of the animal is provided. Also provided are methods for making such animals, and methods of treating animals, including humans, with antibodies or antisense directed to GDF-11. The animals so treated are characterized by increased muscle tissue and bone tissue.
US20080275042 4-Phenyl-5-Oxo-1,4,5,6,7,8-Hexahydroquinoline Derivatives for the Treatment of Infertility The present invention relates to 4-phenyl-5-oxo-1,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R1 is (1-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R2, R3 are independently halogen, (1-4C)allyl, (2-4C)alkenyl, (2-4C)-alkynyl, (1-4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R4 is phenyl or (2-5C)-heteroaryl, both substituted with R7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkylthio and (di)(1-4C)-alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydro-quinoline derivatives in therapy, more specifically for the treatment of infertility
US20080279870 ALK protein tyrosine kinase, cells and methods embodying and using same The present invention provides for a transgenic animal model that constitutively expresses a protein encoded by the NPM-ALK gene in lymphoid tissue, and exhibits enhanced and accelerated development of a T cell lymphoproliferative disorder or B cell plasma cell tumor, together with the identification of cells transduced with the ALK tyrosine kinase gene or fusion proteins thereof, and methods for using this animal model and cells for screening compounds or treatments for antitumor activity. In preferred embodiments, the animal is a transgenic mouse that expresses a human NPM-ALK gene operably linked to human regulatory sequences, and the cells of the mouse have at least one copy of the NPM-ALK transgene, whereby the mouse constitutively expresses a protein encoded by the NPM-ALK transgene. The animals and cells of the invention are useful in the study of NPM-ALK-dependent lymphomagenesis and plasma cell tumors and in the development of treatments for these conditions.
US20100034744 Method For Screening Anti-HIV Drugs and A Diagnostic Method of AIDS The present invention elucidated the interaction between host-side factors and HIV particles, and provided a method for screening anti-HIV-1 drug targeting a new host-side factor. Furthermore, the present invention provided a new diagnostic method of AIDS based on the interaction.
CN103420940A Aralkyl naphthenic aminopiperazine derivatives and applications thereof as multi-targeted antidepressant The invention discloses aralkyl naphthenic aminopiperazine derivatives and applications thereof as a multi-targeted antidepressant. The derivatives are compounds which are shown as the formula (VIII), or medicinal salts thereof. Compared to the clinically-used conventional antidepressants and antidepressants with single action mechanism, the aralkyl naphthenic aminopiperazine derivatives have the advantages of better curative effect, wider adaption diseases, and smaller toxic and side effects.
CN101921250A Bisabolane sesquiterpene derivative and preparation method and application thereof The invention relates to a bisabolane sesquiterpene derivative, a preparation method thereof and applications thereof as an antimicrobial agent. The preparation method comprises the following steps: firstly carrying out strain culture on Aspergillus sp. of Dichotella gemmacea in a strain culture medium; and then carrying out fermentation culture in a fermentation culture medium, filtering liquid generated from fermentation, removing thallus, and extracting obtained fermentation liquor through an organic solvent; concentrating extracted liquor, carrying out column chromatography or thin layer chromatography chromatographic separation; and concentrating obtained eluent to obtain colorless crystal, namely the bisabolane sesquiterpene derivative. In the invention, the bisabolane sesquiterpene derivative has the function of inhabiting the activity of pathogenic bacteria and can be used as the antimicrobial agent, in addition, the raw materials can be used for mass production, and the application prospect is wide.
US20080227756 Administering a bisphosphonate until the bone mineral density is within a normal range, interrupting administration to enable the development of the sectional momentum of inertia, and resuming administration when the bone mineral density falls by 5-10% of the normal range This procedure consists in the first stage, of the administration of enough quantity of bisphosphonate preparation during the necessary period of time to acquire a degree of volumetric mineral density of the cortical tissue of application, within the normal range (average.±.1 DS). Then the administration of the bisphosphonate preparation is interrupted in order to enable the development of the sectional momentum of inertia. The length of the second stage can be determined by means of a tomography. That is to say, that the periods of administration or non-administration of the mineralizing agent are defined or controlled by precise osteologic variables and therefore are not fixed. If during the second stage the cortical mineral density drops by 6-10% of the maximum value previously obtained, administration of bishphosphonate preparation should be resumed until the corresponding maximum adjusted value is reached again. The proposed procedure of a period with bisphosphonate followed by another period without the bisphosphonate agent improves fracture resistance, provided that the length of both periods is controlled by defined osteologic variables.
US20120095081 Treatment of paraoxonase 1 (pon1) related diseases by inhibition of natural antisense transcript to pon1 The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Paraoxonase 1 (PON1), in particular, by targeting natural antisense polynucleotides of Paraoxonase 1 (PON1). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of PON1.
CN103054892A Gracillin-hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof The invention relates to a gracillin-hydroxypropyl-beta-cyclodextrin inclusion compound and a preparation method thereof. The inclusion compound comprises hydroxypropyl-beta-cyclodextrin and gracillin. The ratio of the amount of the gracillin-hydroxypropyl-beta-cyclodextrin is 1:10-20. The inclusion compound is prepared through the following steps of respectively dissolving the gracillin and the hydroxypropyl-beta-cyclodextrin in a proper amount of absolute ethyl alcohol, stirring until the gracillin and the hydroxypropyl-beta-cyclodextrin are completely dissolved, mixing two absolute ethyl alcohol solvents and placing the two absolute ethyl alcohol solvents in a heating magnetic stirrer for an inclusion reaction when the ratio of the amount of the obtained gracillin-hydroxypropyl-beta-cyclodextrin after drying is 1:10-20, and obtaining gracillin-hydroxypropyl-beta-cyclodextrin inclusion compound power after drying when the reaction is finished. The gracillin-hydroxypropyl-beta-cyclodextrin inclusion compound and the preparation method thereof can remarkably improve solubility of the gracillin, prepared inclusion compounds are high in inclusion rate and good in stability, and preparation of peroral preparations or injection preparations is easy to achieve.
US20110183963 Amino Acid Conjugates of Quetiapine, Process for Making and Using the Same The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.
EP1515707A2 Method of treating atherosclerosis and other inflammatory diseases The present invention is directed to methods utilizing vascular endothelial growth factor receptor (VEGFR) antagonists to treat atherosclerosis and other inflammatory diseases.
US20100081677 Heteroarylamide pyrimidone derivatives The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.
CN1927313A Pharmaceutical composition for treating pharyngitis The invention relates to a medicinal composition using crude herbs as the essential component for treating pharyngitis, which comprises the following raw materials (by weight portion): honeysuckle flower 400-500, radix scrophulariae 300-400, belamcanda rhizome 300-400, adenophora root 300-400, India trumpetflower 200-280, menthol 6-12. The preparation according to the invention can be prepared in the form of capsules, tablets, granules or pills.
WO2006051270A1 5-heteroaryl thiazoles and their use as p13k inhibitors The invention provides thiazole derivatives of formula (I), or pharmaceutically acceptable salts thereof in which Ring A, R1, R2 and R3 are as defined in the specification; a processes for their preparation; pharmaceutical compositions containing them; and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.
US7396837 topoisomerase I inhibitors; stimulate topoisomerase I-mediated DNA cleavage and their cytotoxic potential; antitumor agent; prostate gland, ovaries, colon cancer; marine alkaloids New lamellarins are provided of the general formula III or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof
EP1531832B1 Therapeutic compositions for use in prophylaxis or treatment of diarrheas The invention provides a therapeutical composition comprising purified fractions of compounds being or containing a pathogen-inhibiting oligosaccharide sequence for use as a medicament. The present invention especially describes an oligosaccharide-containing substance or receptor binding to diarrheagenic Escherichia coli and/or zoonotic Helicobacter species, and use thereof in, e.g., pharmaceutical, nutritional and other compositions for prophylaxis and treatment of conditions due to the presence of Escherichia coli and/or zoonotic Helicobacter species. The invention is also directed to the use of the receptors for diagnostics of Escherichia coli and/or zoonotic Helicobacter species.
US20100196380 Babesia Subtilisin Provided is an isolated and purified protein produced by a naturally occurring Babesia sp. comprising an amino acid sequence at least 90% identical to SEQ ID NO:1 and an isolated and purified nucleic acid encoding the above protein. Additionally provided is an isolated and purified nucleic acid comprising at least 20 nucleotides having a sequence 100% identical to a portion of SEQ ID NO:2 or its complement. Further provided is an antibody preparation comprising an antibody that specifically binds to the above protein. Also provided are methods of diagnosing a Babesia sp. infection in a mammal, methods of determining whether a blood preparation is contaminated with a Babesia sp., methods of determining whether a blood preparation is contaminated with a Babesia sp., and methods of treating a mammal infected with a Babesia sp., the method comprising inhibiting the production or activity of the protein comprising an amino acid sequence at least 90% identical to SEQ ID NO:1 by the Babesia sp. in the mammal. Additionally provided are methods of screening a compound for treating an infection by a Babesia sp.
WO2011118778A1 Cell proliferation suppression agent and method for screening same Disclosed is a cell proliferation suppression agent that is also effective for androgen-independent prostate cancer. The cell proliferation suppression agent contains as an active ingredient a function inhibiting substance or an expression inhibiting substance of antisense RNA (CTBP-AS) expressed at the vicinity of an androgen receptor (AR) binding site of a C-terminal binding protein (CTBP1) gene.
CN101289450B Tyrosine phthalocyanines derivates, preparation thereof and applications in preparation of photodynamic drugs The invention relates to a tyrosine phthalocyanine derivative which has a structural general formula, in the formula, M is equal to Zn or Al, R is equal to H, Na or CH2CH3. The preparation method for the tyrosine phthalocyanine derivative is: (1) an intermediate II is obtained through the reaction of tyrosine and 4-nitrophthalic nitrile with protected amino group; (2) an intermediate III can be obtained by detracting Boc in the solution of dichloromethane and trifluoroacetic acid; (3) the tyrosine phthalocyanine derivative I can be obtained by cyclizing of the dinitriles intermediate that comprises the tyrosine; wherein, the Boc is di-tert-butyl dicarbonate, a DMF is N, N-dimethylformamide, and a DBU is 1,8-diazacyclo(5,4,0)hendecene-7. The invention also comprises the application of the tyrosine phthalocyanine photosensitizers in preparing photodynamic medicines.
CN103405429A VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2) inhibitors and use thereof The invention relates to the field of medicinal chemistry, and in particular relates to compounds (1-32) and a medical use of pharmaceutical compositions comprising the compounds, in particular to a use of the compounds as VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2) kinase inhibitors.
EP1611121B1 Pyridazinone derivatives as cdk2-inhibitors The present invention relates to novel pyridazinone derivatives of the general formula (I), wherein A is A1 or A2; O A1= ~,N~R A2= NH R H O R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl (C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1,-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-Cio alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.
CN101836998A Application of tyrosol glucoside in preparing anti-hemorrhagic shock drug The invention relates to an application of tyrosol glucoside in preparing an anti-hemorrhagic shock drug, and the tyrosol glucoside is tyrosol heteroside or tyrosol galactoside. The research results of relative pharmacological tests on the tyrosol heteroside show that the tyrosol heteroside and tyrosol galactoside have obvious hemorrhagic shock resistant activity, particularly have remarkable activity in resisting hypovolemic shock seawater soaking wounds caused by wounds, and can serve as an anti-hemorrhagic shock drug.
CN102307861A Phenylimidazole compounds To provide a pharmaceutical product (chemotherapeutic agent) effective in the prevention and treatment of hyperlipidemia, obesity, etc. A phenylimidazole compound represented by the following General Formula (1): wherein, R1 represents a hydrogen atom, a phenyl lower alkyl group optionally having a substituent, or a pyridyl lower alkyl group optionally having a substituent, and the benzene ring and the pyridine ring are optionally substituted with 1 or 2 substituents selected from the group consisting of halogen atoms, cyano group and halogen-substituted lower alkyl groups. One of R2 and R3 represents a hydrogen atom and the other represents a lower alkoxy group. R4 represents a phenyl group optionally having a substituent. R5 and R6 are the same or different, and represent a hydrogen atom or a lower alkyl group. R7 and R8 are the same or different, and represent a hydrogen atom or a lower alkoxy group. However, when R1 represents an unsubstituted phenyl lower alkyl group, R2 represents a lower alkoxy group, R3 represents a hydrogen atom, R4 represents a phenyl group optionally having a substituent, and R5 represents a hydrogen atom, R6 is not a hydrogen atom.
EP1208103B1 Reverse-turn mimetics and methods relating thereto Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having structure (I) are disclosed, wherein A, R1, R2, R2a, R3, R3a and R4 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.
US20090105192 Glycosaminoglycans derived from k5 polysaccharide having high anticoagulant and antithrombotic activities and process for their preparation Glycosaminoglycans derived from K5 polysaccharide having high anticoagulant and antithrombotic activity and useful for the control of coagulation and as antithrombotic agents are obtained starting from an optionally purified K5 polysaccharide by a process comprising the steps of N-deacetylation/N-sulfation, C5 epimerization, O-oversulfation, selective O-desulfation, 6-O-sulfation, N-sulfation, and optional depolymerization, in which said epimerization is performed with the use of the enzyme glucoronosyl C5 epimerase in solution or in immobilized form in the presence of divalent cations. New, particularly interesting antithrombin compounds are obtained by controlling the reaction time in the selective O-desulfation step and submitting the product obtained at the end of the final N-sulfation step to depolymerization.
EP2505201A1 Trmp5 inhibitors support body weight reduction without reducing food intake The present invention relates to the field of weight management and the prevention and/or treatment of metabolic disorders. In particular, the present invention provides a composition comprising at least one Trpm5 inhibitor which is effective in the treatment of prevention of metabolic disorders or risk factors thereof, such as overweightness or obesity, without having to reduce food intake below metabolic needs.
CA2267932C Compositions for postgastrectomic mineral supply An objective of the present invention is to provide compositions for supplying minerals to patients who underwent gastrectomy to thereby treat or prevent postgastrectomic syndrome. The composition for postgastrectomic mineral supply according to the present invention comprises an indigestible oligosaccharide and/or an indigestible sugar alcohol and a mineral.
WO2010109093A1 Water soluble defructosylated pea extract, and use thereof as a prebiotic agent The present invention relates to a water soluble defructosylated pea extract, substantially free of proteins and peptides, as well as to an oligosaccharide composition such as that contained in said extract. The invention also relates to the method for preparing same, and to the use thereof as a prebiotic agent.
US20080214596 Determining the level of expression and/or phosphorylation state of S6;rapamycin; antitumor Disclosed is a method for determining the sensitivity of a proliferate disease in a subject to treatment with an mTOR inhibitor, comprising determining the level of expression and/or phosphorylation state of S6 in a sample derived from the subject, as well as related methods of treatment and uses.
CN102579410A Method for preparing compound ornidazole sustained-release oral ulcer film The invention relates to the field of pharmaceutical preparation, in particular to a method for preparing a compound ornidazole sustained-release oral ulcer film. The pathogenic bacterium of oral ulcer are mainly based on anaerobic bacterium, the clinic treatment of oral ulcer mainly comprises the method of orally taking drugs, because of the influences of drug absorption and first pass effect, the drug local concentration is caused to be low, and the curative effect is not ideal. Xanthan gum is adopted as the compound oral ulcer film of a film-forming material, after the oral pasting drug administration, the compound ornidazole sustained-release oral ulcer film has high antibacterial agent concentration and the functions of slowly releasing, easing pain, diminishing inflammation and promoting ulcer healing, thus having a good clinic application prospect.
US20130011342 Surfactant-free, water-free formable composition and breakable foams and their uses A substantially surface active agent-free and foam adjuvant-free composition which includes a hydrophobic solvent, a wax and a propellant. A substantially surface active agent-free and foam adjuvant-free composition, further comprising, a tetracycline antibiotic, or one or More other active agents. A method of treatment, using a substantially surface active agent-free and substantially foam adjuvant-free composition.
WO2009089361A2 Systems methods and formulation for topically treating nail fungal infection and nail psoriasis The present invention is drawn to systems, methods, and formulations for treating nail disorders. The system comprises an active agent formulation and a first barrier film. The active agent formulation includes an active agent and an aqueous liquid component. The first barrier film is configured to form a sheath over at least a portion of a finger or toe on which the nail is located. An optional second barrier film, with lower moisture vapor transmission rate than the first barrier film, is placed between the first barrier film and the active agent formulation (or between the active agent formulation and the external environment) to reduce the water evaporation from the active agent formulation. The sheath is configured to be capable of securing and retaining the active agent formulation within the sheath on a finger nail or toe nail while reducing evaporation of the liquid component of the aqueous liquid component of the active agent formulation. The active agent formulation can be a 'slow-molding' hydrogel formulation that can slowly flow into the exact shape of the diseased nail to assure intimate contact and continuous delivery of the drug, while cannot be squeezed out of the position during the application.
CN101353333A 10- deacetylate-9(R)-hydrogenization-1-deoxypaclitaxel analogue and preparation thereof The invention relates to a 10-deacetylbaccatin-9(R)-hydrogenation-1-deoxidized paclitaxel analog and a preparation method thereof. The structural formula of the analog is as the right; in the method of the invention, 1-deoxidized baccatin VI is taken as a material for synthesizing the 1-deoxidized paclitaxel analog. The method of the invention maintains the ring skeleton and the necessary functional group of taxanes and selects the taxanes as a semi-synthetic precursor or carries out structure decoration on the taxanes; the obtained output 10-deacetylbaccatin-9(R)-hydrogenation-1-deoxidized paclitaxel analog has the biological activity of antitumor of the natural paclitaxel and has a certain application prospect in the aspects of reducing the multidrug resistance and the side effects of the natural paclitaxel. The method has the advantages of easily obtained materials, simple and convenient operation, good selectivity and high yield.
CN1957933A Application of theanine in preparing medication of curing sequela of apoplexy or convalescent period of apoplexy An application of theanine in preparing the medicine and health-care food for preventing and treating apoplexy sequela and apoplexy restory period is disclosed.
CN103142476A Calcitriol suspension and preparation method thereof The invention relates to a calcitriol suspension and a preparation method thereof. The suspension is prepared from the following ingredients in percentage by weight: 0.0005% of calcitriol, 1.4-1.8% of meglumine, 15-20% of polyethylene glycol 400, 1.5-2.5% of polyethylene glycol 6000, 2.0% of suspending agent, 8.0% of wetting agent and the balance of distilled water. According to the suspension, the content of calcitriol is remarkably increased, so that the drug dosage is reduced; and the stability of calcitriol to light and air is improved, and the bioavailability of calcitriol is also remarkably improved.
EP2259782A1 Pharmaceutical formulations of resveratrol and methods of use thereof for treating cell disorders A method of inducing NAD+ synthesis in a subject. The method comprises administering to the subject a therapeutically effective amount of resveratrol or a functionally equivalent analogue or derivative thereof. NAD+ synthesis increases the activity of Poly(ADP-ribose) polymerase (PARP) enzymes and sirtuin enzymes. The PARP enzyme is PARP-1 or PARP-2 and the sirtuin enzyme is selected from the group consisting of SIRT1, SIRT2, SIRT3, SIRT4, SIRT5, SIRT6 and SIRT7.
CN102718793A Phenyltin coordination compound and preparation method and application thereof The invention discloses a phenyltin coordination compound, and a preparation method and application thereof. The structural formula of the phenyltin coordination compound is figured as follows, wherein Ph represents phenyl. The preparation method comprises the following steps: adding 1 mmol of N-hydroxy-3,4,5,6-tetrachlorophthalimide, 1.0-1.5 mmol of sodium ethoxide, 1-1.5 mmol of diphenyltin oxide and 20-30 ml of methanol into a container; at the temperature of 50-70 DEG C, stirring and refluxing for 6-7 hours; cooling to the room temperature, and evaporating to obtain an orange solid; and recrystallizing the orange solid with dichloromethane-ethanol to obtain a yellow transparent crystal, namely an organic tin coordination compound, wherein the volume ratio of the dichloromethane to the ethanol is 2:1-1:1. The phenyltin oxide coordination compound is applied to preparation of medicines for treating leukemia, lung adenocarcinoma and colon cancer. The organic tin coordination compound has the characteristics of high anticancer activity, good lipid solubility, low cost, simple preparation method and the like and provides a new way for developing anticancer medicines.
CN101396439A Manufacture method of powder capable of quickly removing five gornorrheas The invention discloses a manufacturing method of powder for rapidly eliminating five types of painful urinary dribbling. The use of the method can eliminate five types of painful urinary dribbling within a plurality of days. The manufacturing method is realized by the following technical proposal, Japanese climbing fern spore, costustoot, twotooth achyranthes root, Chinese angelica and rhubarb are put in a drying box for drying, the time is 5-10 hours, the temperature is 40-60 DGE C, the water content is not more than 5 percent, when in processing of fine powder with 300 meshes, realgar is frozen at minus 10 DEG C for 3 days and then removed out, thereby processing into the fine powder with 300 meshes; the powder is combined together for stirring for 20 minutes, and finished product powder is obtained by bottling.
WO2013113074A1 Combination therapy comprising a growth hormone variant and an oligonucleotide targeted to the growth hormone receptor The present disclosure relates to a method for treatment or prevention of diseases have an increased level of insulin-like growth factor I (IGF-I). The method comprises administration of a growth hormone (GH) variant having antagonistic activity in combination with an oligonucleotide targeted to growth hormone receptor (GHR) to a subject in need.
CN1919206A Vitexin injection and oral administration preparation thereof The invention relates to a Vitexin injection or oral administration preparation for treating cardiovascular diseases and process for preparation, wherein each 1000ml of the Vitexin injection comprises Vitexin 0.1-100g, each 1000 dosage units of the oral administration preparation comprises Vitexin 0.1-100g, and medicinal supplementary materials comprises diluent, flow aid, auxiliary solvent, excipient and osmoregulation agent.
US7241782 Modifications are prepared by subjecting an alkaline solution of torasemide to a rapid acidification with inorganic or organic acids at 0 to 35 degrees C. The invention relates to a novel polymorph V of torasemide, to a process for its preparation, to its use as a raw material for the preparation of crystalline modifications I and III of torasemide, to amorphous torasemide modifications and to pharmaceutically acceptable salts of torasemide, to pharmaceutical forms containing the said novel polymorph V of torasemide as the active ingredient as well as to its use.
EP2061476A2 Compositions containing cdp-choline, and methods of use thereof The present invention is directed to methods of improving memory, learning, cognition, synaptic transmission, and synthesis and release of neurotransmitters and increasing brain phospholipid levels in a subject, comprising administering to the subject a CDP-choline or a pharmaceutically acceptable salt thereof.
US20110229446 Method and composition to relieve sexual discomfort and improve vaginal health A method to reduce sexual discomfort for a woman during sexual intercourse vaginally introduces a lubricant composition comprising carrageenan comprising 0 to 92% by weight iota carrageenan, 10% to 100% by weight lambda carrageenan, and, 0 to 18% by weight kappa carrageenan; water such that the ratio of carrageenan to water is in the range of 1:10 to 1:50; at least one prebiotic; and, a natural humectant with a peak tackiness force of less than 50 g and a work of adhesion of less than 0.500 GS.
EP1721613A1 Hesperidin for the treatment of epilepsy, migraine, schizophrenia, depression and drug abuse Use of hesperidin and/or its aglycon hesperetin or their salts to prepare a medicine or nourishment supplement to prevent and/or treat epilepsy. - ACTIVITY : Anticonvulsant; Antimigraine; Neuroleptic; Antidepressant; Antiaddictive; CNS-Gen. - MECHANISM OF ACTION : None given.
EP1460999B1 Methods of making and using theaflavin, theaflavin-3-gallate, theaflavin-3'-gallate and theaflavin 3,3'-digallate and mixtures thereof The present invention discloses methods of making a mixture of theaflavin-3-gallate, theaflavin-3'-gallate and theaflavin 3,3'-digallate, pharmaceutical compositions of the above mixture of theaflavins, diet supplement compositions of the above mixture of theaflavins and methods for using the above mixtures of theaflavin and pharmaceutical compositions thereof to treat or prevent various diseases. The present invention also discloses methods of making theaflavin, theaflavin-3-gallate, theaflavin-3'-gallate and theaflavin 3,3'-digallate, each as a separate compound, pharmaceutical compositions of the above compounds, diet supplement compositions of the above compounds and methods for using the above compounds to treat or prevent various diseases.
US7034045 Monofluoroalkyl derivatives The present invention provides certain monofluoroalkyl derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
CN102038740A Formula for treating aphtha The invention discloses a formula for treating aphtha, comprising the following components at the ratio: 5.5-6.5 of mung bean and 3.5-4.5 of mirabilite. The preparation method of the formula comprises the following steps of: respectively grinding the mung bean and the mirabilite; screening with a sieve of 100 meshes; mixing and stirring by the ratio of 5.5-6.5:3.5-4; and storing in a container. A patient takes 4-6g of formula at every time and three times a day. The formula has the effective effect that the formula for treating aphtha can be prepared by oneself, which is convenient.
EP2025338A1 New medicaments for the treatment of chronic ostructive pulmonary disease The use of 2-(N-(1,1-dimethyl-omega -phenyl-alkyl)-amino)-1-(6-hydrox y-4H-benz-(1,4)-oxazin-3-on-8-yl)-ethanol derivatives (I) for treating chronic obstructive pulmonary disease (COPD) is new. The use of benzoxazinonyl-ethanolamine derivatives of formula (I) (including individual optical isomers, enantiomer mixtures and racemates) or their acid addition salts is claimed in the production of medicaments for treating chronic obstructive pulmonary disease (COPD). [Image] n : 1 or 2; R 1>, R 2>H, alkyl, halo, OH or alkoxy; R 3>H, alkyl, OH, halo, alkoxy, carboxyalkoxy or alkoxycarbonylalkoxy; alkyl moieties have 1-4C. Independent claims are included for: (a) inhalable pharmaceutical formulations containing (I); and (b) new benzoxazinonyl-ethanolamine derivatives of formula (I') (including optical isomers, salts etc.). [Image] n : 1; R 1>', R 2>' : H or alkyl; R 3>' : alkyl, OH, alkoxy, carboxyalkoxy or alkoxycarbonylalkoxy; and provided that: (1) alkyl moieties have 1-4C; and (2) if R 1> and R 2> are both ortho-methyl, then R 3> is not OH. - ACTIVITY : Antiinflammatory. - MECHANISM OF ACTION : beta -Mimetic.
US20130059806 Epigenetic co-repressors of the gamma-globin gene and methods of using same This disclosure describes methods of screening for compounds that disrupt the interaction between DNMT1 and the gamma-globin promoter or between LSD-1 and the gamma-globin promoter. This disclosure describes methods of screening for compounds that de-repress the gamma-globin gene.
EP1063999B1 Epiallopregnanolone in the treatment of cns disorders The use of epiallopregnanolone (3 beta -hydroxy-5 alpha -pregnan-20-one) for the treatment of inter alia steroid induced mood disorders and CNS disorders is disclosed. Further, the use of epiallopregnanolone for the manufacture of pharmaceuticals is disclosed, together with a list of symptoms suitable for treatment with epiallopregnanolone or pharmaceuticals comprising the same.
CN102497853A Dry powder formulations and methods for treating pulmonary diseases The present invention is directed toward respirable dry particles for delivery of divalent metal cation salts and/or monovalent cation salts to the respiratory tract and methods for treating a subject having a respiratory disease and/or infection.
US20120202787 Novel Heteroaryl Imidazoles And Heteroaryl Triazoles As Gamma-Secretase Modulators Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I; as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
EP2776445A1 Therapeutically active thiazolo-pyrimidine derivatives A series of thiazolo[5,4-d]pyrimidine derivatives of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof: (I) Q represents a group of formula (Qa), (Qb), (Qc), (Qd) or (Qe) are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
CN103520730A Chitosan oligosaccharide nanoparticle capable of loading hydrophobic anti-tumor medicine The invention discloses a chitosan oligosaccharide nanoparticle capable of loading a hydrophobic anti-tumor medicine. When a conjugate, which is formed by coupling chitosan oligosaccharide with high biocompatibility and biodegradability with an antalgic medicine ibuprofen, is dispersed in water, the hydrophobic ibuprofen is self-assembled to form a core of the nanoparticle, the hydrophilic chitosan oligosaccharide is self-assembled to form a spherical shell, so that the chitosan oligosaccharide-ibuprofen nanoparticle is formed. The ibuprofen has high hydrophobicity, so that the obtained nanoparticles have small average particle size and are distributed uniformly. The hydrophobic core of the chitosan oligosaccharide-ibuprofen nanoparticle has a good affinity effect on the hydrophobic medicine, so that when the chitosan oligosaccharide-ibuprofen nanoparticle is used for loading the hydrophobic anti-tumor medicine, the targeting property, the low toxicity and the slow release property of the medicine can be improved. The ibuprofen in the nanoparticle can achieve an antalgic effect.
US20090191260 Aerosol and use thereof The invention relates to an aerosol, in which a phase containing a solid substance is dispersed into a gaseous dispersant. The aim of the invention is to achieve a particularly effective anti-inflammatory action for the treatment of respiratory diseases. According to the invention, a depot is contained in the dispersed phase, said depot releasing silver ions when it comes into contact with water.
US20100105640 Aromatase Inhibitors for Emergency Contraception There is disclosed an emergency contraceptive preparation which comprises at least one aromatase inhibitor wherein the preparation comprises at least one dose for administration on one or more days to a female patient following an unprotected sexual encounter until the establishment or continuation of pregnancy of the patient is prevented. Also disclosed is a method of emergency contraception.
CN103333071A 10-benzylideneanthrone compound and application thereof The invention provides a new 10-benzylideneanthrone compound, and its application in preparation of antitumor drugs. The invention provides the new 10-benzylideneanthrone compound with antitumor activity and its application, especially the compound (I-2) or (I-4) has significant antitumor activity on human ovarian cancer caused by an HO cell strain, thus providing a basis for new drug screening.
CN101422441A Nimesulide sustained-release tablet and preparation method thereof The invention provides a Nimesulide sustained-release tablet and a preparation method thereof. The Nimesulide sustained-release tablet is prepared by Nimesulide, skeleton sustained-release material, a bond and a lubricant. The invention is characterized in that the skeleton sustained-release material is a mixture of compressible starch and hydroxypropyl methylcellulose with the weight ratio of 1 : 1; moreover, the weight ratio of the Nimesulide : the compressible starch : the hydroxypropyl methylcellulose is 2 : 1 : 1; wherein, the preferable viscidity range of the hydroxypropyl methylcellulose is 20 to 4000 mpa.s. The Nimesulide sustained-release tablet can be slowly released to maintain more stable blood medicine concentration and longer action time; the Nimesulide sustained-release tablet taken before sleeping can appear peaking effect in the morning, achieve the best clinic treatment target and have better medicament economy advantage.
US20100137339 Amorphous form of n--n-methyl-acetamide The present invention relates to an amorphous form of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide, methods for its preparation, its use as a therapeutically active agent and pharmaceutical compositions comprising the novel form.
WO2008037266A1 Inhibitors of conventional protein kinase c isozymes and use thereof for treating inflammatory diseases The present invention relates to the use of an inhibitor that inhibits a conventional protein kinase C alpha isozyme and/or of an inhibitor that inhibits a conventional protein kinase C alpha isozyme and that inhibits a conventional protein kinase C gamma isozyme as a medicament or for the preparation of a medicament for treating inflammatory diseases, in particular inflammatory diseases that are mediated by a Toll-like receptor 2 (TLR-2) and/or an Interleukin-1 receptor (IL-1R). The present invention further provides suitable inhibitors for use in the present invention; pharmaceutical compositions and kits for treating such TLR-2 and/or IL-1R mediated inflammatory diseases.
US20120190738 Inhibitors of phosphatidylinositol-3-kinase (pi3) and inducers of nitric oxide (no) The present invention relates to compounds of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention also relates to the use of compound of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention further relates to a method of treating malignancy by inhibition of PI3-Akt pathway and or induction of NO by administration of compound or said composition to a mammal in need thereof.
CN103044408A Itraconazole applied to treatment of malignant tumor or salt thereof and composition thereof The invention relates to itraconazole applied to treatment of gastric cancer, lung cancer and liver cancer, and a composition of the itraconazole. The daily dose of the itraconazole is 0.1-5000mg, and the itraconazole has good curative effect when the daily dose is 200mg. The itraconazole and the composition of the itraconazole disclosed by the invention have the beneficial effects that by subcutaneous injection of the itraconazole solution or the composition, the survival time of high and low-dose groups of SPF-grade Konmin mice that have liver cancer H22 can be prolonged. The itraconazole or the composition of the itraconazole has obvious inbibitional effect on Lewis lung cancer of mice in comparison with the control group according to the influence on subcutaneous tumor of the Lewis lung caner, the growth rate (P(0.01) of the tumor can be slowed down; the size (P(0.01) of the tumor is reduced; and the tumor control rate is respectively 43.0% and 45.6% after the treatment is ended. The itraconazole or the composition of the itraconazole influences positive staining of the human gastric cancer tissue VEGF (Vascular Endothelial Growth Factor) in cell cytoplasm, and the VEGF positive expression of a 0.9% sodium chloride solution group is obviously higher than that of the itraconazole group (P(0.05).
CN1931871A New triterpene saponin componds with anticancer activity The present invention relates to new triterpene saponin compound with anticancer activity. The triterpene saponin compound is separated from giantleaf ardisia rhizome as one botanical medicinal material and possesses obvious in vitro anticancer activity. It may be applied in preparing antitumor medicine.
CN102379842A Preparation method for fleroxacin injection The invention discloses a preparation method for a fleroxacin injection. The method comprises the following steps of: a, treating a container with 0.2 percent by volume of ethylene diamine tetraacetic acid solution; b, weighing fleroxacin, dissolving with an acetic acid-sodium acetate buffering solution in an amount of 25-35 percent based on the total volume, adding water for injection to a labeled amount, and introducing nitrogen for protecting; and c, performing split charging in the hundred-level purified environment. The method has the advantages of simple process, small quantity of auxiliary materials and stable and good product quality.
CN101703521A Application of montmorillonite in preparing drugs The invention relates to new application of montmorillonite, in particular to application of montmorillonite in drugs for treating acute and chronic pharyngitis and tonsillitis. The dosage form of the clinically applied preparation is montmorillonite gel or montmorillonite powder or montmorillonite nasal lotion. The invention explores new application of the medical montmorillonite and opens up a new application field.
EP2560616A2 Artificial tear emulsion The present invention relates to an oil-in-water emulsion comprising at least one mucomimetic polymer, at least one lipid of phospholipid type, at least one lipid other than the phospholipid, at least one stabilizing polymer, and a hydrophilic liquid, to an emulsion comprising an aqueous phase that contains at least one stabilizing polymer and at least one mucomimetic polymer, and an oily phase that contains at least one lipid of phospholipid type and a lipid other than the phospholipid, to a medicament comprising one of these emulsions, and to the use of one of these emulsions as an agent for restoring and/or replacing the lachrimal film or as a carrier for an active compound.
CN1899302A Oral sticking plaster preparation for treating oral ulcer and its preparing method The present invention discloses a kind of oral sticking plaster for treating oral ulcer and its preparation process. The oral sticking plaster is prepared with montmorillonite as main medicinal material 500 weight portions, carbomer 15 -35 weight portions, aspartame 0.1-2 weight portions, vanillin 0.1-1.5 weight portions, ethanol solution of 85 % concentration as wetting agent 250-450 weight portions. Compared with available technology, the present invention has the features of long effective duration, high treating effect, simple preparation process, convenient use, etc.
US20130012480 Crystalline salts of (4s,4as,5ar,12as)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide and methods of using the same A crystalline mono hydrochloride salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide is disclosed having improved stability. In addition, a crystalline mono mesylate salt and crystalline mono sulfate salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide are also disclosed having improved stability. A pharmaceutical composition containing the crystalline salts and methods of treating inflammatory skin disorders and bacterial infections comprising administering the crystalline salts are also disclosed.
WO2005123088A1 Solid orally ingestible formulations of tetrodotoxin The present invention refers to an outwardly solid or completely solid ( or designed to be orally ingested)composition of tetrodotoxin and/or analogs or derivatives thereof. The tetrodotoxin present in this composition can be in the form of a racemate, as a mixture of stereoisomers or as a pure stereoisomer. The composition can be in the form of a tablet, a capsule, a drop or a dragee. It can comprise a gastroenteric coating and be formulated as an immediate release formulation or as a controlled release formulation. The tetrodotoxin composition is used for the treatment of pain.
US20090220498 Method for Discovering Inhibitors of the Epstein-Barr Virus-Induced Gene 3 (EBI3) and Derivatives Thereof for the Treatment of Metastasizing Tumors and Allergic Asthma The present invention relates to a method for identifying inhibitors of the Epstein Barr virus-induced gene 3 (EBI3), a method for producing a pharmaceutical composition, comprising an inhibitor, a respective pharmaceutical composition and a method for treating a metastasizing tumor disease or allergic asthma, comprising the administration of an effective amount of an inhibitor of EBI3.
US20090074786 Formulations for treating ocular diseases and conditions Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; non-dispersed mass-forming liquid formulations which form a gel or gel-like substance in an aqueous medium; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration, or wet age-related macular degeneration in a subject. The liquid formulations may comprise rapamycin or other therapeutic agents.
CN103169723A Preparation method and application of oleanolic acid disaccharide saponin component The invention relates to a preparation method of an oleanolic acid trisaccharide saponin component 3-O-alpha-L-rhamnopyranose-(1 arrow 2)-alpha-L-arabinopyranose oleanolic acid saponin and application of the component for resisting tumors. The invention also relates to application of an extract which is from rhizomes of Pulsatillachinensis(Bunge)Regel and contains the compound for resisting the tumors. The tumors include lung cancer, liver cancer, gastric cancer, colon cancer, glioma, breast cancer, cervical cancer, leukemia, lymph cancer and the like.
US20090005454 Method of Reducing Nosocomial Infections Nosocomial infections, particularly nosocomial infections of intubated patients, are reduced by applying a liquid disinfectant directly to the mucosa, before intubation, by a swab applicator or by a spray applicator.
WO2014076261A1 Sulphated polysaccharide composition The invention concerns a composition made from at least one sulphated polysaccharide, in particular from an algae, and combined with at least one food ingredient. This composition can be used, in particular, in the field of food or in the treatment or prevention of an infection caused by microsporidia in humans or animals. It has useful properties as an antiparasitic agent in humans or animals; for the treatment or prevention of an infection caused by at least one microsporidia in humans or animals; in particular for the treatment or prevention of an infection caused in bees by the microsporidia Nosema, preferably Nosema ceranae or Nosema apis, or indeed for stimulating the immune defences of bees.
CN102335164A Application of 5,6,7,4'-tetrahydroxy flavone and derivatives thereof in preparation of drugs for preventing and treating hyperuricemia and gout The invention relates to the field of medicines, and particularly discloses application of 5,6,7,4'-tetrahydroxy flavone and derivatives thereof in preparation of drugs for preventing and treating hyperuricemia and gout. The invention also provides capsules and sustained-release tablets for preventing and treating hyperuricemia and gout. The invention discovers that 5,6,7,4'-tetrahydroxy flavone and derivatives thereof have strong anti-gout action, can significantly reduce the serum uric acid level of mouse suffering from hyperuricemia at low dosage, have activity equivalent to that of allopurinol, have low toxic and side effects, have safety higher than that of anti-gout drugs such as colchicine, allopurinol and anturan used clinically at present, can be used for preparing drugs for preventing and treating hyperuricemia and gout, and have broad clinical application prospects.
US20130005813 Compounds and their Salts Specific to the PPAR Receptors and the EGF Receptors and their Use in the Medical Field The present invention relates to compounds comprising the general formula (I), in which R1 and R2, which may be identical or different, are selected from the group comprising —H or a linear or branched alkyl group having from 1 to 6 carbon atoms or together form an aromatic or aliphatic ring with 5 or 6 atoms; Y and Z, which may be identical or different, are selected from the group comprising —H, —OH, —COOH, —OR3, —CH(OR3)COOH, in which R3 is selected from H, phenyl, benzyl, —CF3 or —CF2CF3, vinyl, allyl and a linear or branched alkyl group having from 1 to 6 carbon atoms.
EP1517892B1 Ring-substituted diphenyl azetidinones, method for the production thereof, medicaments containing said compounds, and use thereof Disclosed are ring-substituted diphenyl azetidinones of formula I, a method for the production thereof, medicaments containing said compounds, and the use thereof for treating hyperlipidemia, arteriosclerosis, and hypercholesterolemia.
US20090048336 Escitalopram oxalate powders Escitalopram oxalate powders having definite particle size distribution parameters, processes for preparing the powders, and solid pharmaceutical formulations containing the powders.
CN103393936A Drug for preoperative intervention of induced labor in late pregnancy The invention discloses a drug for preoperative intervention of induced labor in late pregnancy, and aims to solve the problem of gut purge before the induce labor in late pregnancy. The drug is characterized by being composed of following raw materials by weight: horseweed herb, cassiabarktree fruit, ternate buttercup root, caulis trachelospermi, asarum caulescen, polygonatum kingianum, psoralea corylifolia, dried orange peel, flower of sunflower, turbo cornutus solander, plant soot, and magnesium sulfate. The characteristic of good gut purge effect of the drug when the drug is used before the induced labor in late pregnancy has been testified by clinical tests, and the drug is worthy for being promoted and applied to the clinic.
CN103655564A Method of inhibiting constitutively active phosphorylated FLT3 kinase The present invention includes a method of inhibiting or reducing deregulated FLT3 tyrosine kinase activity or FLT3 tyrosine kinase expression in a subject with a proliferative disease by administering to the subject having or suspected to have the proliferative disease, a therapeutically or prophylactically effective amount of the compound of Formula I: or pharmaceutically acceptable salt thereof.
US20050182002 Killing Burkitt's lymphoma cell or a chronic lymphocytic leukaemia cell The present invention relates to a method of inducing cell death in a neoplastic cell expressing a serotonin transporter (SERT) such as Burkitt's lymphoma cell or a chronic lymphocytic leukaemia cell. The method comprising exposing said neoplastic cell to a therapeutically effective amount of a pharmaceutically active agent which interacts with said SERT, said therapeutically effective amount being sufficient to cause death of said neoplastic cell.
CN103432480A Medicinal power for treating erosion-type tinea pedis and preparation method of medicinal power The invention discloses medicinal power for treating erosion-type tinea pedis and a preparation method of the medicinal power. The medicinal power is prepared from the following raw materials in parts by weight: 30-100 parts of radix sophorae flavescentis, 30-100 parts of cortex dictamni, 30-100 parts of common cnidium fruit, 30-100 parts of fructus kochiae, 30-100 parts of rhizoma smilacis glabrae, 30-100 parts of cortex phellodendri, 30-100 parts of common carpesium fruit, 30-100 parts of cortex pseudolaricis, 30-100 parts of dried alum and 30-100 parts of yam rhizome. The preparation method of the medicinal power is that the radix sophorae flavescentis, the cortex dictamni, the common cnidium fruit, the fructus kochiae, the rhizoma smilacis glabrae, the cortex phellodendri, the common carpesium fruit, the cortex pseudolaricis, the dried alum and the yam rhizome are ground into extremely-fine power together and then stored in a bottle/bottles for later use after being disinfected under high pressure. The invention has the benefits as follows: the medicinal power can directly act on diseased regions, fully brings the functions of excreting dampness, clearing heat and killing funguses to relieve itching into play, and has the effect of skin protection. Compared with other medicines for treating the erosion-type tinea pedis, the medicinal power is indeed practical and innovative.
US20070293457 Boron-containing small molecules as anti-inflammatory agents Methods of treating anti-inflammatory conditions through the use of boron-containing small molecules are disclosed.
EP1228046B1 Phthalazinone derivatives as pde 4 inhibitors The compounds of formula (I) in which R1, R2, A, B and Ar have the meanings as given in the description are novel effective PDe4 inhibitors.
EP1507528A2 Methods for using jnk inhibitors for treating or preventing disease-related wasting The present invention relates to methods useful for the treatment or prevention of disease-related wasting. The methods of the invention comprise the administration of an effective amount of a JNK Inhibitor. In one embodiment, the disease is HIV, AIDS, cancer, end-stage renal disease, kidney failure, chronic heart disease, obstructive pulmonary disease or tuberculosis. The methods can further comprise the administration of a therapeutic or prophylactic agent useful for the treatment or prevention of HIV, AIDS, cancer, end-stage renal disease, kidney failure, chronic heart disease, obstructive pulmonary disease, chronic infectious diseases (e.g., osteoarthritis and bacterial endocarditis), chronic inflammatory diseases (e.g., scleroderma and mixed connective tissue disease) or tuberculosis.
CN1879627A A sustained release injection containing cephalosporin and application thereof The invention relates to a release injection which contains cefradine, wherein it is formed by release micro ball and dissolvent; the release micro ball contains release findings and penicillin antibiotic; the dissolvent is the special one contains sodium carboxymethyl cellulose as suspension agent; the viscosity is 100cp-3000cp (20Deg. C-30Deg. C); the release agent is selected from EVAc, polyphenyl, PLA, PLGA, sebacic acid polymer, protein pastern, and dope; the release micro ball can be made into release implant agent; the release implant agent and release injection is laid on bacteria stove or injected, to release the medicine for 5-30 days, to keep the effective medicine density and reduce the whole toxicity. The invention can be used to cure the infection caused by staphylococcus, streptococcus, etc.
EP2289522A1 Mixture of hyaluronic acid for treating and preventing peptic ulcer and duodenal ulcer The present invention is related to a hyaluronic acid composition with a binary mixture of hyluronic acids having mainly different weight-average molecular weight and then different rheological, scaffold and degradation properties in aqueous solution. The resulted compositions have demonstrated an optimal balance between adhesion, tissue scaffold and treating time to the peptic and duodenal ulcer and bleeding. Thus, the present inventive binary mixture exhibits a quick and lasting effect on the treatment and prevention of duodenal or peptic ulcer and bleeding which is very good thing indeed.
WO2009104988A1 Pharmacological adjuvants based on coordination compounds of d-metals The invention relates to the use of small and ultra small quantities of bi- and oligo-nuclear forms of the coordination compounds of d-metals in the form of drugs or agents for enhancing the therapeutic efficiency of pharmacological substances.
CN103520207A Targeting cisplatin sodium nano-alginate liposome The invention relates to a targeting cisplatin sodium nano-alginate liposome. The targeting performance of the targeting cisplatin sodium nano-alginate liposome is embodied by that the liposome is modified by targeting molecules, and the liposome has the grain diameter of about 100nm and is composed of phosphatidylcholine, cholesterol, sodium alginate, an anti-tumor drug cisplatin and targeting molecules. The liposome has a high systematic cisplatin carrying rate (15.24%) and a high encapsulation rate (89.92%), can be subjected to specific combination with targeting molecules on surfaces of tumor cells so as to achieve toxicity attenuation and synergism, and is locally and specifically applied to the preparation of drugs for tumor treatment. Particularly, the liposome has more excellent anti-tumor activity to oophoroma resisting.
WO2011096642A2 Pharmaceutical composition for preventing and treating inflammatory diseases The present invention relates to a pharmaceutical composition for preventing and treating inflammatory diseases, containing 2-[2-chloro-6-(3-iodobenzyl)-furyn-9-yl]-tetrahydro-thiophene-3,4-diol (LJ-1888) or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition according to the present invention has a remarkably low toxicity compared with a known A3 adenosine receptor agonist or antagonist, and is thus useful for preventing and treating inflammatory diseases.
US7189706 C2,5′-disubstituted and N6,C2,5′-trisubstituted adenosine derivatives and pharmaceutical compositions containing them The present invention concerns novel C2,5′-disubstituted and N6,C2,5′-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in the treatment and prophylaxis of diseases and disorders affected by adenosine receptor agonists.
US20090258861 Tetrahydronaphthyridine Derivatives The present invention relates to tetrahydronaphthyridine derivatives of the general formula (I): or of the general formula (I′) in which A and R1 are as defined within, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, including the treatment diseases mediated by H3 ligands, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
WO2013174854A1 Terpene extract for the treatment of hair loss The present invention refers to a composition comprising cucurbitacins and their glucoside derivatives, wherein cucurbitacins D, I, L. and A and their glucoside derivatives are present, as a whole, in terms of percentage by weight, in an amount greater than 25% of the total weight of the cucurbitacins and their glucoside derivatives, and wherein cucurbitacins B, E and the derivative o f cucurbitacin E, ecballic acid, are each present at a concentration below 2.5% of the total weight of the cucurbitacins and their glucoside derivatives, for its use in the treatment or prevention of hair loss.
US20080139601 3-Cyano-Quinoline Derivatives With Antiproliferative Activity The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
EP2252688A1 Synthetic phosphodiester oligonucleotides and therapeutical uses thereof A composition of phosphodiester oligonucleotides of various defined sizes has been created that mimics the effects of defibrotide. The composition essentially consists of mixtures of synthetic phosphodiester oligonucleotides comprising Nmers ranging from 40 mers to 65 mers. The phosphodiester oligonucleotides are preferably heteropolymers composed of either A, G, C, and T at each position but may also be homopolymers, i.e. the same base may be present at each position in the oligonucleotide. These mixtures are effective in the treatment of cancer and other diseases.
WO2006062481A1 New benzofuran derivatives and their use in the treatment of obesity, type ii diabetes and cns disorders . The present invention relates to compounds of the general Formula (I), wherein R1, R2 and R3 are as defined in the description; to pharmaceutical compositions comprising these compounds; and to the use of the compounds for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes, and/or CNS disorders.
WO2009112155A1 Heteroaryl-substituted dicyanopyridines and use thereof for treatment of cardiovascular diseases The present application relates to new heteroaryl-substituted dicyanopyridines having formula (I), to a method for the production thereof, to the use thereof for treatment and/or prevention of diseases and also the use thereof for production of pharmaceuticals for treatment and/or prevention of diseases, preferably for treatment and/or prevention of cardiovascular diseases.
CN101048382B New indole or benzimidazole derivatives The present invention relates to compounds of the formula (I), wherein R<1> to R<7>, X and Y are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compoundsare useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.
WO2007142139A1 Method of identifying candidate for remedy of acute myeloid leukemia It is intended to disclose a method of identifying a candidate for a remedy of acute myeloid leukemia which comprises contacting activated mutant FLT3 with Lyn in the presence of a test substance and examining whether or not the test substance inhibits the binding of activated mutant FLT3 to Lyn and/or whether or not the test substance inhibits the phosphorylation of Lyn in a cell expressing activated mutant FLT3. It is also intended to disclose a method of identifying a candidate for a remedy of acute myeloid leukemia which comprises contacting a test substance with a cell expressing Lyn and examining whether or not the test substance inhibits the expression or Lyn and/or whether or not the test substance inhibits the phosphorylation of STAT5 by Lyn. A substance identified by the above method is useful as the active ingredient of a remedy for acute myeloid leukemia.
WO2006062434A1 Modified 5'- phosphonate azidothymidine-potential anti-viral preparations The invention relates to molecular biology, virology and medicine, in particular to novel 3'azido-3'-dezoxythymidine-phosphonates of general formula (I), wherein R is alkyl groups including groups containing halogen atoms, carboxy, hydroxy, alkoxy and acyloxy- groups and substituted aminocarbonyl groups. The inventive compounds can be used in the form of anti-viral agents since they are low-toxic, efficiently inhibit the reproduction of a type 1 immunodeficiency virus in the culture of MT-4 cells and generate azidothymidine in mammal organisms, thereby ensuring the gradual increase thereof in blood.
US20090304758 Formulations of lipoic acid and hyaluroinc acid and/or the derivatives thereof in the pharmaceutical and cosmetic fields The present invention relates to novel formulations comprising lipoic acid and hyaluronic acid and/or the derivatives thereof for use in the repair of chronic ulcers, the regeneration of damaged skin, the prevention of skin aging and, when administered by the systemic route, to treat peripheral neuropathies and intoxications by chemical and/or biological agents.
EP2627653A1 3 -amino- pyrazole derivatives useful against tuberculosis A compound of Formula (I) or a pharmaceutically acceptable salt thereof: (I), Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, -CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicylic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
US7977506 Amino acid for delivering active materials; bioavailability Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
CN1629147A Pyrazinamide bulk drug and pyrazinamide tablet The invention discloses a pyrazine amide raw material medicament and pyrazine amide tablet for treating tuberculosis, which is prepared from 2-cyano pyrazine, purified water and sodium hydroxide through hydrolysis reaction, hydrolyse mother liquor concentration, refining, drying, disintegrating, and mixing. The invention can be applied for the production of tablet, injection, transfusion, oral liquid and capsule of anti-tuberculosis medicament.
EP2357184A1 Imidazoquinoxaline compounds as immunomodulators The invention provides novel compositions comprising imidazoquinoxaline compounds of formula (I). Also provided are the compounds of formula (I) for use in methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and the compositions for use in methods of administering the compositions in combination with (an) other agent(s).
US20070249587 Aromatic-Ring-Fused Pyrimidine Derivative There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.
WO2008064756A3 Use of substances reducing cellular glutathione content for producing a medicament for treating t-cell mediated autoimmune diseases The invention relates to the use of substances reducing cellular glutathione content for producing a medicament for treating T-cell mediated autoimmune diseases. The substances are selected from the group comprising L-BSO, ifosfamide, diethyl maleate, acetaminophen or other glutathione-S conjugating agents.
US20090176872 Carotenoid Composition and Method for Protecting Skin A method for protecting skin against damages caused by ultra-violet (uv) radiation from the sun, comprising administering to a subject in need of protection an effective amount of a composition containing lycopene from a natural source and one or more carotenoid selected from among phytoene and phytofluene or mixtures thereof.
WO2012139529A1 D-amino acid oxidase inhibitor for preventing and/or reversing opioid tolerance Provided are a D-amino acid oxidase inhibitor for preventing and/or reversing opioid tolerance, and a method using the D-amino acid oxidase inhibitor for preventing and/or reversing opioid tolerance. Also provided are a method for using the D-amino acid oxidase inhibitor for preventing and/or treating pain, and a method for identifying a compound for preventing and/or reversing opioid tolerance.
EP2274303A1 Processes for preparing sunitinib and salts thereof Methods for preparing sunitinib or salts thereof are described using novel intermediates of formula (I); wherein X is either Cl or imidazole.
US20080076803 Antimicrobial preservative comprising a mixture of 1,2-benzisothiazolin-3-one, pyrithione or salts thereof, and an alkalinizing agent to bring the pH to 11 or higher; free of ethylenediamine and N-alkylisothiazolin-3-one; water solubility; high stability at various temperatures, clear concentrates The invention relates to microbicidal preparations which comprise a) at least one of 1,2-benzisothiazolin-3-one and its derivatives, b) at least one of 2-mercaptopyridine N-oxide, its salts and derivatives and c) at least one alkalinizing agent, or which are prepared by mixing components a) to c), where the preparations have a pH of at least 11. The preparations are characterized by the fact that they are clear and storage-stable, and they are suitable for use as preservatives.
CN102940608A Tripterine controlled-release solid dispersion The invention provides a tripterine controlled-release solid dispersion taking stearic acid modified nano CaCO3 as a carrier.
EP1844034A1 Dnt-fumarate and methods of preparation thereof (S)-N,N-Dimethyl-3-(l-naphthalenyloxy)-3-(2-thienyl)propanamine fumarate (DNT-fumarate) and polymorphs of DNT-fumarate, compositions of DNT-fumarate and its polymorphs, processes for the preparation of DNT-fumarate and its polymorphs, and processes for the preparation of duloxetine hydrochloride from DNT-fumarate are provided.
US20080194571 Acetylenic Piperazines as Metabotropic Glutamate Receptor Antagonists The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, B, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR 5 mediated disorders.
US7538123 Indole derivative having piperidine ring The present invention relates to a compound represented by the following formula, a pharmacologically acceptable salt thereof, or a use thereof as a pharmaceutical: wherein R1 and R2 are substituents adjacent to each other, and together with two carbon atoms to each of which they attach, form a 5- to 7-membered non-aromatic carbocyclic group or the like, which may be substituted by 1 to 4 substituents selected from (1) an oxo group, (2) a hydroxyl group, and the like; R3 represents a hydrogen atom or the like; and R6 represents a hydrogen atom or the like. This compound has a superior strength of binding to a 5-HT1A receptor and an antagonism to the receptor, and is useful as an agent for treating or preventing lower urinary tract symptoms, and particularly symptoms regarding urinary storage.
US20130040976 Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
CN103610849A Application of renqingchangjue (Chinese character) in preparation of drug for treating prostatic cancer The invention discloses application of renqingchangjue (Chinese character) in preparation of a drug for treating a prostatic cancer. The renqingchangjue is a name of a drug recorded in 2010 edition of the People's Republic of China pharmacopoeia, is a Tibetan prescription, and is prepared from more than 100 drugs such as pearl, cinnabar, sandalwood, dalbergia wood, agilawood, fructus chebulae, calculus bovis, muskone and stigma croci. The renqingchangjue has the functions of clearing away heat and toxic materials, and reconciling and nourishing the body. By adopting the renqingchangjue, the technology biases in the application aspect are overcome. A pharmacological experiment shows that a petroleum ether extract of the renqingchangjue has a good inhibiting effect on a prostate cancer cell in vitro; the effect is equivalent to or slightly better than that of cis-platinum; medicated serum bodies of a plurality of extracts of the renqingchangjue also have significant inhibiting effects on the prostatic cancer in vitro.
US20100210648 Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
US20120295934 New Hexahydrocyclopentapyrrolone, Hexahydropyrrolopyrrolone, Octahydropyrrolopyridinone and Octahydropyridinone Compounds The invention provides novel compounds having the general formula (I) wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used for the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.
EP1718322B1 Synergistic compositions with fk-228 An antitumor agent containing, in combination, at least one kind of antitumor agent selected from the group consisting of an antitumor agent that forms a cross-link with DNA and shows an antitumor effect, an antimetabolite antitumor agent and a taxane antitumor agent, and a histone deacetylase inhibitor. According to the present invention, an antitumor agent causing reduced side effects and having a superior antitumor activity can be provided.
CN101904837A Use of rotenone as non-small cell lung cancer cell sensitizer The invention relates to novel use of a mitochondrial respiratory chain inhibitor rotenone in reversing the tolerance of non-small cell lung cancer cells to targeted antineoplastic agents. The rotenone serves as a non-small cell lung cancer cell sensitizer and can reverse the tolerance of the non-small cell lung cancer cells to the targeted antineoplastic agents. The invention shows the combination of rotenone compounds and TRAIL has no obvious toxic or side effect on normal cells and is a novel medicinal composition used for treating the non-small cell lung cancer.
CN1562061A Tylan phosphate granular agent and its preparing method A granular tylosin phosphate is prepared through thermally dissolving medical adhesive in non-salt water, dissolving tylosin phosphate in water, proportionally mixing them together, mixing with basic material chosen from corn starch, soybean powder, zeolite, pearlite, etc, spray drying and sieving.
CN102020574A diisopropylphenyl gamma-aminobutyrate derivatives and preparation methods thereof The invention discloses diisopropylphenyl gamma-aminobutyrate derivatives, water soluble compounds (II) formed by salification of the derivatives and acids and preparation methods thereof. In the invention, the compounds (II) are formed by using diisopropylphenol (1) as a raw material. The water soluble compounds have a general formula (II), wherein R may be hydrogen atom, methyl, ethyl, n-propyl, isopropyl, n-butyl and isobutyl; and HB represents an acid which can be used as a medicine. The water soluble compounds disclosed in the invention, after hydrolyzing in vivo, can form the 2,6-diisopropylphenol (I) which has an esthetic effect, so the compounds can be used as a preanesthetic medicine for injection.
CN102872016A Medicine combination A medicine combination is prepared by mixing memantine hydrochloride, huperzine B, huperzine A and pharmaceutically acceptable auxiliary materials, wherein the memantine hydrochloride, the huperzine B and the huperzine A serve as active pharmaceutical ingredients. The medicine combination can be used for treating sequelae of brain infarction and various dementia.
CN1882547B 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors The present invention provides compounds of formula (I) and compounds of formula (I), (VII-a), as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R, R and X have defined meanings.
US20110305774 Treatment of retroviral reservoirs exploiting oxidative stress Activation of HIV-1 replication causes oxidative stress, which in turn potentiates HIV-1 replication. The common basis for the compounds of the present invention is: A) the capacity of reactivating HIV-1 from latency, and B) the ability to counteract the cellular machinery which activates in order to limit the effects of oxidative stress. In this way, oxidative stress can be potentiated and a “chain reaction” is sparked. This “chain reaction” induces a more efficient reactivation of HIV-1 from latency and, in some cases, induces selective killing of the infected cells. Actions A) and B) can either be carried out by one drug exerting both effects, or obtained by the combined use of distinct drugs. There are two main cellular machineries counteracting oxidative stress, i.e. the thioredoxin (Trx) thioredoxin reductase (TrxR) system and glutathione. Herein, we present drug strategies capable of exerting action B) by blocking either of the two machineries.
US20110028413 Methods of Reducing Methotrexate Nephrotoxicity The present invention provides compositions and methods to reduce renal damage caused by nephrotoxic drugs such as methotrexate. The invention provides compositions comprising a substituted cyclodextrin, methotrexate and a pharmaceutically acceptable carrier, where the cyclodextrin is present in an amount effective for substantially inhibiting the nephrotoxic effect of the methotrexate.
EP1387685B1 Analgesic composition comprising an opioid and a sodium channel blocker A pharmaceutical analgesic composition comprising an opioid analgesic agent and a compound that binds to the SS1 or SS2 subunit of a sodium channel, such as tetrodotoxin and saxitoxin, and analogs thereof. Administration of an opioid analgesic agent and a compound that binds to the SS1 or SS2 subunit of a sodium channel, such as tetrodotoxin and saxitoxin, and analogs thereof, produces analgesia in the treatment of pain in mammals.
CN101947253A External compound preparation for curing tinea corporis as well as preparation method and content measuring method thereof The invention relates to an external compound preparation for curing tinea corporis as well as a preparation method and a content measuring method thereof, which solves the problems of slow therapeutic action and low curative ratio of the existing oral and injective therapy techniques in curing tinea corporis, tinea cruris, hand-foot tinea and other fungus infection diseases and the difficulties of the existing oral and injective therapy techniques that more factors and defects influence the product quality in the product production process. The external compound preparation of the invention is prepared by the following steps: dissolving benzoic acid, salicylic acid, iodine, potassium iodide, menthol and borneol with ethanol; and then respectively preparing into tinctures, linimentum, pigmentum, liniment, patch, ointment, gels, lotion, film agents and spray. In the preparation process, a closed preparation method is adopted, thereby preventing active components from volatilizing and ensuring the curative effect of drugs. The invention adopts the convenient and stable content measuring method, thereby ensuring the product quality, enabling the curative effect to be more definite, being capable of curing superficial fungus infection and having good effect for the tinea corporis, the tinea cruris and the hand-foot tinea.
CN1586589A Ginseng stem and leaf total saponin oral disintegration tablet and its preparing method The present invention relates to oral disintegrated tablet of ginseng stem and leaf total ginsenoside for invigorating spleen and nourishing vital energy and its preparation process. Ginseng stem and leaf total ginsenoside as main material as well as stuffing, disintegrating agent, corrective, flow assistant, lubricant and other supplementary material are prepared into the oral disintegrated tablet. Into the supplementary material, adhesive, coating material and/or effervescent agent may be added, if necessary. The oral disintegrated tablet of the present invention has excellent crushing degree, fast disintegration, good taste and low cost, and may be taken with no water and high curative effect.
US20100063073 Methods and Compositions Utilizing Quinazolinones Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.
US20100004187 Cobalt-amine based metal complex as an antibacterial compound Disclosed herein is a method of: administering to a subject suspected of being infected with a bacterium, a composition of a cobalt (III) compound having the formula CoR1R2R3R4R5R6 or a salt thereof and an antibiotic compound. Each of R1, R2, R3, R4, and R5 is the same or different and includes an N-based ligand donor atom selected from the group consisting of ammonia, primary amine, or secondary amine, or salt thereof. R6 is a ligand. Also disclosed herein is a composition of the above cobalt (III) compound and an antibiotic compound. Also disclosed herein is a method of administering the above cobalt (III) compound to a subject diagnosed as needing a broad spectrum antibiotic
US7629456 Modified L-nucleic acid The present invention relates to a modified L-nucleic acid, comprising a L-nucleic acid part and a non-L-nucleic acid part, whereby the L-nucleic acid part is conjugated to the non-L-nucleic acid part and the conjugation of the L-nucleic acid part with the non-L-nucleic acid past leads to a slowed elimination out of the organism, in comparison with a L-nucleic acid which only comprises the L-nucleic acid part, said L-nucleic acid part being a spiegelmer.
US20120039806 Compounds and Methods for Modulating an Immune Response The present invention relates to the identification of proteins which bind the dendritic cell marker known as Clec9A. The present invention provides new compounds for targeting therapeutic agents such as antigens to dendritic cells. Also provided are methods of modulating a humoral and/or T cell mediated immune response to the antigen, methods of delivery of a cytotoxic agent to dendritic cells thereof involved in diseased states, methods of modulating the uptake and/or clearance of cells with a disrupted cell membrane, cells infected with a pathogen, dying cells or dead cells, or a portion thereof, and methods of modulating antigen recognition, processing and/or presentation, as well as immune responses to material derived from cells with a disrupted cell membrane, cells infected with a pathogen, dying cells or dead cells, or a portion thereof.
CN101417060A Plaster capable of treating trauma, traumatic injury, alopecia areata and burn and scald The invention relates to a salve for the treatment of traumatism, contusion, alopecia areata as well as burn and scald, essentially solving the problems that drugs for curing traumatism, contusion, alopecia areata as well as burn and scald have single function, poor curative effects, easy wound infection and scars at the wound after recovery. The salve is characterized in that the salve is prepared by drugs according to the following weight ratio: 3 portions to 5 portions of calomeas, 8 portions to 10 portions of realgar, 8 portions to 12 portions of calamine, 5 portions to 9 portions of boswellia carteri, 5 portions to 9 portions of myrrh, 3 portions to 4 portions of borneol, 8 portions to 12 portions of resina draconis, 5 portions to 9 portions of catechu and 180 portions to 280 portions of vasogen for medical purposes. The salve has the effects of diminishing inflammation and detoxication, removing slough, heeling wounds, invigorating the circulation of qi and blood, reducing swelling and easing pain, disinfesting insects and eliminating toxic materials, promoting blood circulation and removing blood stasis, removing toxic substance and evacuating pus, promoting reunion of the fractured bones, promoting hair growth, repairing wound, promoting regeneration of skin and quickening tissue regeneration.
EP2201011A2 Novel compounds having indazole frameworks, methods for preparing the same and pharmaceutical composition comprising the same Novel compounds having indazole frameworks, as well as a method for preparing the same and a pharmaceutical composition comprising the same are provided. The compounds of the present invention can inhibit protein kinase activity and thus the pharmaceutical composition of the present invention can be used to prevent or treat diseases or disorders which are related to protein kinase activity.
US7517907 specific activator of retinoic acid receptors subtype beta; 6-[3-adamantan-1-yl-4-(2,2-dimethyl[1,3]dioxoian-4-ylmethoxy)phenyl]naphthalene-2-carboxylic acid; useful in human or veterinary medicine; for body/hair hygiene, treating acne-prone skin, promoting hair regrowth, limiting hair loss, dry skin Novel ligand compounds having the structural formula (I): and the salts and optical/geometrical isomers thereof are suited for formulation into pharmaceutical compositions useful in human or veterinary medicine, or, alternatively, into cosmetic compositions.
CN101747384B 5-chlorine salicylyl hydrazine triphenyltin chloride coordination compound, as well as preparation method and application thereof The invention discloses a 5-chlorine salicylyl hydrazine triphenyltin chloride coordination compound, the structural formula of which is shown as follows. The preparation method of the coordination compound comprises the following steps of: adding 1.5-2.0mmol of N-1,8-dinaphthalene acyl-5-chlorine salicylyl hydrazine, 3-4mmol of sodium methylate and 50mL of absolute methanol into a 100ml round bottomed flask, and stirring for 0.5h; then adding 2.0-3.0mmol triphenyltin chloride; and after stirring at normal temperature for 6h, transferring the solution into a reaction kettle; crystallizing at 150-170 DEG C for 100-120h; and then cooling to room temperature at the speed of 5 DEG C/h to obtain a yellow crystalloid which is an organic tin coordination compound, wherein the yield is 70-80 percent. The organic tin coordination compound has higher anti-cancer activity, can be used as a raw material to prepare the medicines for treating liver cancers and cervical cancers for people. Compared with traditional commonly-used platinum-based anti-cancer medicines, the invention has the characteristics of higher anti-cancer activity, good fat solubility, low cost, simple preparation method and the like.
US20080058366 Daytime and nighttime dosages; anticholinergic agents; nonsedating antihistamines A treatment regimen for rhinitis with rhinorrhea includes a daytime dosage unit containing medication for treating rhinitis and an anticholinergic agent for treating rhinorrhea, and a nighttime dosage unit containing medication for treating rhinitis and an attenuated dosage of anticholinergic agent or no anticholinergic agent. A pharmaceutical package for treating rhinitis with rhinorrhea includes a daytime dosage unit containing a medication for treating rhinitis and an anticholinergic agent for treating rhinorrhea, a nighttime dosage unit containing medication for treating rhinitis and an attenuated dosage of anticholinergic agent or no anticholinergic agent, indicia to distinguish between the daytime dosage unit and the nighttime dosage unit, instructions for coordinating the daytime dosage unit and the nighttime dosage unit as a treatment regimen for treating rhinitis with rhinorrhea, and a unifying container for housing the daytime dosage unit, the nighttime dosage unit, the indicia, and the instructions.
CN101439104A Medicament for treating burn by 'dry, moistening, dressing' three in one bandaging method The invention relates to a medicine for treating burning by three-in-one combination bandaging strapping of 'dryness', 'moist', and 'dressing'. The medicine has the main characteristics that the medicine comprises medicinal powder, dressing and plaster, and is prepared by mainly using purple gromwell root, coptis teeta, bismuth subnitrate tablets, chloramphenicol tablet, rheum officinale, the dried rhizome of rehmannia, forsythia, the root of red-rooted salvia, safflower, angelica, borneol and the like according to according to a certain proportioning. Compared with the traditional treatment method, the medicine can moisten a burn sore surface when the burn sore surface is dry and can dry the burn sore surface when the burn sore surface is moist, can soften, oxidize in proper sequence, can clear away sores, naturally promotes skin so that low degree burn can fast heal and high degree burn does not need skin-grafting. The medicine proved by many cases of clinical trial has precise healing efficacy and high cure rate.
WO2014128198A1 Bilaterally-substituted tricyclic compounds for the treatment of human immunodeficiency virus type-1 (hiv-1) infection and other diseases The invention relates to bilaterally-substituted tricyclic compounds and pharmaceutical compositions containing them, for use as medicaments. Due to their ability to interact with an internal RNA loop and to mimic a protein a-helix these compounds are effective in the treatment and/or prevention of HIV-1 (Human Immunodeficiency Virus-1) infection and other diseases such as those caused by other RNA viruses and by gram-positive and gram-negative bacteria, or infectious or chronic diseases responsive to inhibition of DNA transcription, or infectious or chronic diseases where these compounds can be used to modulate the function of RNA internal loops, or infectious or chronic diseases where these compounds can be used as agonists or inhibitors of a-helical proteins in interaction with other biomolecules.
EP2345649A1 Benzimidazole compound in crystal form and salt thereof The present invention aims to provide a stable form of (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide, which is free of problems of water adsorption and the like, and shows superior water solubility. The present invention provides a crystal and a salt of (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide in a crystal form.
WO2009056256A1 Use of megestrol acetate having improved solubility for the treatment of cancer cachexia The present invention relates to the treatment of cancer patients suffering from cachexia as a co-morbidity with a megestrol acetate formulation (MegaceTM ES) having improved solubility.
WO2008098371A1 Compositions and method for reducing amyloid beta in a mammal The present invention relates to combinations, compositions and methods for reducing amyloid beta (Aβ) intracellular accumulation and/or reducing extracellular Aβ oligomers or Aβ aggregates in a mammal. More particularly, the present invention provides combinations, compositions and methods for treating or preventing Alzheimer's disease.
CN103330681A Glucose injection in inner bag of unsterilized multi-chamber infusion bag and preparation method thereof The invention discloses a glucose injection in an inner bag of an unsterilized multi-chamber infusion bag and a preparation method thereof. The invention also discloses the glucose injection in the inner bag of the sterilized multi-chamber infusion bag. According to the glucose injection in the inner bag of the unsterilized multi-chamber infusion bag, the inner bag comprises at least two independent chambers; at least one chamber is filled with an injection which is easy to oxidize and deteriorate, and at least one chamber is filled with the glucose injection, wherein the content of dissolved oxygen of the glucose injection is limited so that oxidative deterioration of the injection is not caused easily by the dissolved oxygen during sterilization or storage processes of the inner bag.
US20080267961 SOLUBLE ErbB3 AND TREATMENT OF CANCER Regulation of sErbB3 isoforms in methods of regulating heregulin activity or ErbB receptor activities is disclosed. Cancer therapeutics and methods of therapeutically treating cancer comprising sErbB3 are also disclosed. Detection of sErbB3 in biological samples for risk assessment and prevention, screening, diagnosis, prognosis, theragnosis, evaluation of responsiveness to treatment, and/or monitoring of disease progression, recurrence, or metastasis of a cancer is disclosed as well. In examples, sErbB3 nucleic acid sequences, polypeptides, molecular probes, and antibodies are useful agents for regulation, expression, detection, and cancer therapeutics related to sErbB3.
WO2014156462A1 Agent for inducing differentiation of white adipocytes into brown-like adipocytes An agent for inducing the differentiation of white adipocytes into brown-like adipocytes, said agent being characterized by comprising a compound represented by formula (1), which is a product of a cyclization reaction of a hydroxystilbene, or a pharmaceutically acceptable salt thereof. In formula (1), R1 to R8 represent a hydrogen atom, a hydroxy group, a saturated or unsaturated and linear or branched alkoxy group having 1-10 carbon atoms, or a saturated or unsaturated and linear or branched alkyl group having 1-10 carbon atoms, and R1 to R8 may be either the same or different.
US20110107442 Treatment of Male Sexual Dysfunction A composition comprising a selective oxytocin antagonist for use in the treatment and/or prevention of a male ejaculatory disorder; which selective oxytocin antagonist is optionally admixed with a pharmaceutically acceptable carrier, diluent or excipient.
WO2014090173A1 Nanoscale doxorubicin hydrochloride and preparation method therefor A nanosacle doxorubicin hydrochloride particle and a preparation method therefor. The particle uses silica aerogel as a carrier. Doxorubicin hydrochloride is absorbed in pores of the silica aerogel, forming the doxorubicin hydrochloride particle having a diameter of 100 nm or less. The silica aerogel has a porosity of 95-99%, an aperture of 10-50 nm, a specific surface area of 200-1000 m2/g, and a density of 3-300 kg/m3, and the diameters of aerogel particles forming a network are 1-50 nm.
WO2013050426A1 Carbonic anhydrase inhibitor comprising a dithiocarbamate A carbonic anhydrase inhibitor which comprises a compound of general formula: R1R2N-CS2 -M+ for use in the treatment of microbial infection, eye disease or cancer; wherein R1 and R2 are each independently selected from H or an organic substituent, or together form a ring, and optionally contain one or more heteroatoms; wherein R and R2 together comprise at least 5 carbon atoms or at least 2 carbon atoms and a heteroatom, or R2 comprises at least 4 carbon atoms; and wherein M+ comprises a monovalent cation.
US20110160289 Compositions and methods for enhanced sensitivity and specificity of nucleic acid synthesis The present invention relates to nucleic acid inhibitors, compositions and method for enhancing synthesis of nucleic acid molecules. In a preferred aspect, the invention relates to inhibition or control of nucleic acid synthesis, sequencing or amplification. Specifically, the present invention discloses nucleic acids having affinity for polypeptides with polymerase activity for use in such synthesis, amplification or sequencing reactions. The nucleic acid inhibitors are capable of inhibiting nonspecific nucleic acid synthesis under certain conditions (e.g., at ambient temperatures). Thus, in a preferred aspect, the invention relates to “hot start” synthesis of nucleic acid molecules. Accordingly, the invention prevents, reduces or substantially reduces nonspecific nucleic acid synthesis. The invention also relates to kits for synthesizing, amplifying, reverse transcribing or sequencing nucleic acid molecules comprising one or more of the nucleic acid inhibitors or compositions of the invention. The invention also relates to using the inhibitors of the invention to prevent viral replication or treat viral infections in a subject. Thus, the invention relates to therapeutic methods and pharmaceutical compositions using the inhibitors of the invention. The invention thus may be used for in vivo and in vitro inhibition of nucleic acid synthesis and/or inhibition of polymerase activity.
EP2062581B1 The antibiotics composition comprising beta-lactam antibiotics and ionic chelating agents The antibiotics composition comprising at least one of beta-lactam antibiotics and at least one of ionic chelating agents used for inhibiting particulate formation, further comprising at least one of beta-lactamase inhibitors or buffers, or at least one of beta-lactamase inhibitors and buffers simultaneously. The composition can be formulated with at least one of aminoglycoside antibiotics into solution for controlling microbial infection in a container.
CN101697998A Zhenhuang tablet for treating sore throat and ulcer and sore furuncle and preparation method thereof The invention provides a preparation method of Zhenhuang tablet for treating sore throat and ulcer and sore furuncle, and the Zhenhuang tablet is prepared from pearl, artificial bezoar, pseudo-ginseng, extractum radix scutellariae, borneol, pulvis fellis suis and peppermint oil. Compared with the prior art, the preparation of the invention improves the shortages of the original formula and technology, prolongs the quality guarantee period of medicine, improves curative effect and is more suitable for industrial volume production. The preparation of the invention has the efficacy of clearing away heat and toxic material, reducing swelling and easing pain, is used for treating sore throat and ulcer and sore furuncle clinically, has obvious curative effect, convenient use and stable and controllable quality and is worth popularizing and applying clinically.
US20100273748 Antimicrobial therapy Methods and compositions for modulating gene expression and the innate immune response by 1,25(OH)2 vitamin D3 (1,25D3) are provided. Also provided are methods and compositions for modulating histone acetylation using 1,25(OH)2 vitamin D3 (1,25D3).
US7288562 treating diseases or disorders of the respiratory, urinary and gastrointestinal systems This invention generally relates to the derivatives of novel 3,6 disubstituted azabicyclo[3.1.0] hexane's. The compounds of this invention are MUSCARINIC receptor antagonists which are useful, inter-ail for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through MUSCARINIC receptors. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through MUSCARINIC receptors.
WO2005097738A1 Novel sulfonamide derivative Disclosed are a compound represented by the formula (1) below, a prodrug thereof, and their pharmaceutically acceptable salts which have an effect of increasing LDL receptor expression and are useful as drugs for treating hyperlipemia, arteriosclerosis and the like. (1) (In the formula, m, n and p independently represent an integer of 0-4 and 3 ≤ m + n ≤ 8; X represents a group expressed as NR4 or the like; R1, R3 and R4 represent a substituted or unsubstituted aryl group or the like; R2 represents a hydrogen atom or the like; a, b, c, d, e and f respectively represent a hydrogen atom, a substituted or unsubstituted alkyl group or the like; Y represents -SO2- or the like; and Z represents an oxygen atom or the like.)
CN103193859A Dehydroepiandrosterone D cyclobenzo-aminothiazole ring compounds as well as preparation method and application thereof The invention belongs to the field of medicinal chemistry and in particular relates to dehydroepiandrosterone D cyclobenzo-aminothiazole ring imine and imine reducing compounds as well as a preparation method and application thereof. The compounds are shown in a formula I in the specification. An in-vitro antineoplastic activity experiment indicates that the compounds have better broad-spectrum antineoplastic activity, have a favorable inhibition effect on multiple human cancer cells, such as EC109 and EC9706 and are suitable for research of antineoplastic lead compounds or preparation of novel antineoplastic medicaments. The preparation method is simple and convenient and suitable for industrial production.
US20090143457 Polycyclic compounds for use in treating ocular neurodegenerative diseases Described herein are various compounds for treatment of ocular neurodegenerative diseases, including but not limited to glaucoma and diabetic retinopathy. The compounds described herein can act to attenuate and/or block calcium release from external neuronal environments as well as intracellular stores.
US20100069350 New Pyridine Analogues III The present invention relates to certain new pyridin analogues of Formula (I), to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
US20110293562 Use of cardiotrophin-1 for the treatment of metabolic diseases The invention is related to the use of cardiotrophin-1 (CT-1) for the treatment of obesity and associated disorders: hyperglycaemias, insulin resistance, development of type 2 diabetes and dyslipemias and given its anorexigenic role, fat oxidation stimulant, hypoglycaemic, sensitizing agent of the action of insulin on a skeletal muscle level and inhibitor of the intestinal transport of glucose by enterocytes.
US8486451 Adsorption and release of nitric oxide in metal organic frameworks Disclosed are metal organic frameworks that adsorb nitric oxide, NO-loaded metal organic frameworks, methods of preparing the NO-loaded metal organic frameworks, methods of releasing the nitric oxide into a solution or into air, and uses of the metal organic frameworks.
WO2009049961A3 New no-donor aspirin derivatives The present invention refers to new NO-donors aspirin derivatives, a process for their preparation and pharmaceutical compositions containing them.
CN102198200A Quick-acting swelling-diminishing and pain-relieving tincture The product provided by the invention has the advantages that: the medicinal raw materials are readily available; the price is low; the preparation is simple and convenient; the effectiveness is quick; and the treatment effect is obviously. Patients with traumatic injury, sprain lumbago and rheumatic arthralgia rather than bone fracture and skin injury can rub the swelling and aching parts with absorbent cotton impregnated with the product disclosed by the invention, namely quick-acting swelling-diminishing and pain-relieving tincture, for 3 to 5 minutes; at first, the patients may feel fatigue, swelling, numbness, pain and the like, but 10 minutes later, the pain is relieved or diminished; and one day layer, the skin in the swelling part shrinks and the red and swelling symptoms disappear gradually. The patients are required to rub the affected parts with the absorbent cotton impregnated with the tincture twice in the morning and in the evening each day.
WO2014060959A1 Crystalline pemetrexed dipotassium process The present invention provides crystalline pemetrexed dipotassium hemiheptahydrate (I) - characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 29° peaks selected from the XRPD peak set of 5.00, 13.70, 14.90, 15.20, 16.90, 20.00, 20.50, 21.40, 23.6, 24.2, 25.10, 27.5 and 28.30 ± 0.20 29°, DSC isotherm comprising the endothermic peaks ranging between 65 to 85°C (Peak -1), 86 to 105°C (Peak -2), 120 to 132°C (Peak -3), 250 to 265°C (Peak -4), and IR absorption characteristic peaks at approximately 2936 cm-1, 2857 cm-1, 1396 cm-1, 1184 cm-1, 1158 cm-1, 1092 cm-1, 1076 cm-1, 819 cm-1 and 788 cm-1 useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer. The invention also provides process for preparing pemetrexed dipotassium hemiheptahydrate (I) and its pharmaceutical composition thereof.
WO2012115480A2 Diaminopyrimidine derivatives and processes for the preparation thereof The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
US20050054731 Includes a biguanide hypoglycemic agent, a lipid lowering agent, a blood pressure lowering agent and, preferably, an anti-platelet agent A multi-system therapy which is adapted to treat diabetes, metabolic syndrome and obesity includes a hypoglycemic agent, a lipid lowering agent, a blood pressure lowering agent and, preferably, an anti-platelet agent. The composition can further include various vitamins and supplements such as vitamin B6, vitamin B12, arginin, a folate and other vitamins and minerals. Preferably, the hypoglycemic agent is a biguanide hypoglycemic agent without any additional hypoglycemic agent, making the composition suitable for treatment of individuals who are not hyperglycemic as well as those who are hyperglycemic.
CN101952243A 4-dimethylaminobutyric acid derivatives This invention relates to novel 4-dimethylaminobutyric acid derivatives of the formula (I) wherein A1, A2, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.
US20080044476 Peripherally administered viscous formulations Viscous formulations and methods of using such compositions, useful for intramuscular and intra-articular injection are provided to treat peripheral conditions. Such compositions can include triamcinolone particles present in a therapeutically effective amount, a viscosity inducing component, and an aqueous carrier component. The compositions have viscosities of at least about 10 cps or about 100 cps at a shear rate of 0.1/second. In a preferred embodiment, the viscosity is in the range of from about 80,000 cps to about 300,000 cps. In a most preferred embodiment, the viscosity is in the range of from about 140,000 cps to about 280,000 cps at a shear rate of 0.1/second at 25° C. The compositions advantageously suspend the triamcinolone particles for prolonged periods of time.
US20080044403 Immune Markers Used for Diagnosis and Therapy in Connection With Transplant Reactions The invention relates to immune markers for detecting inflammations, immune reactions, and particularly transplant tolerance or transplant reactions, a method for detecting transplant reactions or tolerance, and the use of immune markers for medical prophylaxis, clinical monitoring of progress, transplant follow-up treatment, clinical diagnosis and/or therapy in connection with cell transplants, tissue transplants, or organ transplants.
CN1582905A Use of emodin in preparation of antagonistic TGF beta-1 and medicines to prevent tissues from fibrosis An application of the archin in preparing the medicine for suppressing TGF beta-1 and preventing the tissue fibrosis caused by TGF beta-1 is disclosed.
CN1870983B Compositions and foods for improving lipid metabolism It is intended to provide compositions and foods usable in treating, preventing or improving diseases or symptoms which can be treated, prevented or improved by activating PPAR, in particular, insulin resistant diabetes and hyperlipidemia. Namely, medicinal compositions usable in treating, preventing or improving diseases or symptoms which can be treated, prevented or improved by activating PPAR which contain humulones, isohumulones or lupulones or pharmaceutically acceptable salts or solvates thereof.
US20080214614 reduces intraocular pressure; primary open-angle glaucoma; effective to influence the actomyosin interactions by leading to cellular relaxation and alterations in cell-substratum adhesions The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
EP2632456A1 Composition and method for influencing energy metabolism and treating metabolic and other disorders A composition and method for influencing energy metabolism and treating metabolic and other disorders is provided. A terpenoid lactone that is a selective activator of SIRT1 is generally in the form of a terpenoid dilactone having a 5-alkenyloxy-furan-2- one group, such as strigolactone, GR 24, or another strigolactone analog, and is used as a therapeutic agent in a method for influencing energy metabolism and treating metabolic and other disorders. The terpenoid lactone may be administered as an individual agent or combined with a second compound such as a flavonoid, chalconoid, tannin, or nicotinamide inhibition antagonist.
US20110230534 Composition For Local Anesthesia An object of the present invention is to provide a composition for local anesthesia to be added to a local anesthetic drug, the composition showing a sustained local anesthetic effect and having high safety. The object is achieved by a composition for local anesthesia including a drug antagonistic to a systemic action of adrenaline, i.e., an α2 receptor agonist. The α2 receptor agonist can be added to a local anesthetic agent together with adrenaline or a salt thereof to reduce the amount of adrenaline to be added as compared to that of adrenaline or a salt thereof alone. As a result, a sustained local anesthetic effect is obtained and local anesthesia can be performed with high safety.
CN102492004A Preparation method and application of 2-(4-beta-D-allose pyranoside-phenyl)-2,3-dihydroquinoline-4(1H) and 2-(4-(2,3,4,6-tetrabenzyl)-beta-D-allose pyranoside-phenyl)-2,3-benzodihydropyran The invention relates to a preparation method and an application of 2-(4-beta-D-allose pyranoside-phenyl)-2,3-dihydroquinoline-4(1H) (1) and 2-(4-(2,3,4,6-tetrabenzyl)-beta-D-allose pyranoside-phenyl)-2,3-benzodihydropyran (2). The invention discloses helicide derivatives with a central nervous system improving function, and a preparation method thereof. The compounds provided by the invention have good sedative, sleep-promoting, and convulsion-inhibiting functions. The compounds are collected in a Year 2000 version of Pharmacopoeia of PRC with a medicine name of helicide tablets. The helicide derivative novel medicines are represented by chemical formulas (1) and (2), wherein R1 can be hydrogen and acetyl, and R2 can be semicarbazide, hydroxylamine, and methoxylamine. Acording to the helicide derivatives provided by the invention, a plant active monomer helicide with sedative, sleep-promoting, and convulsion-inhibiting functions is adopted as a matrix compound, structural modification is carried out according to a medicine efficacy molecular principle, and compounds with high activities for improving central nervous system functions are designed and prepared.
WO2014139161A1 Novel high penetration drugs and their compositions thereof for treatment of parkinson diseases One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
CN101264061A Super-critical anti-solvent preparation for water-soluble nano camptothecin powder The invention relates to a supercritical anti-solvent preparation method of water-soluble nanoparticlization camptothecin powder, which is characterized in that, starting CO2 high-pressure pump, injecting CO2 in a high-pressure crystallizing reactor at a flow speed of 5L/h to 20L/h, stabilizing the temperature of the high-pressure crystallizing reactor between 32 DGR C and 75 DGR C, stabilizing the pressure between 7.5MPa and 25MPa, reaching a supercriticality; injecting DMSO or DMF solution with a camptothecin concentration of 1mg/ml to 5mg/ml in the high-pressure crystallizing reactor at a flow speed of 1ml/min to 30ml/min through a nozzle with a pore diameter of 20um to 1000um, dissolving out camptothecin powder with an average grain diameter of 100nm to 800nm, making CO2 circulate in the high-pressure crystallizing reactor for at least half an hour to dry the formed nanoparticlization camptothecin powder; separating DMSO or DMF solution from CO2 in a separation reaction in a pressure of 5MPa to 6.5MPa at temperature of 25 DGR C to 50 DGR C, recycling and reusing DMSO or DMF, making CO2 circulate directly for use. The nanoparticlization camptothecin powder has the advantages of smooth surface, uniform particle size distribution, good water solubility, no solvent remnant, non-pollution manufacturing technique, low cost, high yield, and easy industrialization.
CN102671003A Zhuifengtougu capsules and preparation method thereof The invention provides Zhuifengtougu capsules. The Zhuifengtougu capsules are prepared from the following components by weight: 48.1g of prepared common monkshood mother root, 48.1g of prepared nutgrass galingale rhizome, 48.1g of ligusticum wallichii, 48.1g of Chinese ephedra, 48.1g of prepared kusnezoff monkshood root, 24g of large-leaved gentian, 24g of Chinese angelica, 48.1g of red phaseolus bean, 48.1g of notopterygium root, 48.1g of red paeony root, 48.1g of wild ginger, 48.1g of prepared pedate pinallia jackinthepulpit rhizome, 48.1g of angelica dahurica, 48.1g of licorice root, 24g of roasted large-head atractylodes rhizome, 9.6g of prepared myrrh, 24g of prepared frankincense, 48.1g of earthworm, 96.2g of tuckahoe, 24g of cassia twig, 24g of tall gastrodia tuber, 24g of nardostachyos root and rhizome, 24g of divaricate saposhnikovia root and 38.5g of cinnabar. The medicine is quick in response and good in curative effect, and particularly has the obvious curative effects on wind-cold, dampness pain, quadriplegia, nervous numbness, numbness of limbs and the like.
CN101475554B 1',2',3',7'-tetrahydrotheaflavine-3,3'-digallate, and preparation and use thereof The invention provides a novel compound, which is 1',2',3',7'- tetrahydro theaflavin-3,3'- digallic acid ester and the chemical structural formula thereof is shown as (2). The compound of the invention can be obtained by hydrogenating and reducing theaflavin derivate TF3, has the functions of inhibiting the activity of reverse transcriptase and the activity of HIV gp41 forming a six-strand helical core structure, can prevent HIV virus from entering a host cell, and has stronger inhibiting functions on the activity of the reverse transcriptase and the activity of HIV gp41 forming the six-strand helical core structure than TF3.
WO2007104898A3 Method for reducing the odour caused by lipoamino acids in topical cosmetic and/or pharmaceutical formulations The invention relates to a topical cosmetic and/or pharmaceutical formulation, characterised in that it comprises, based on 100 % of the mass thereof: between 0.05 and 10 mass % of a compound of formula (I), or a salt thereof, or a mixture of said compounds of formula (I) or the salts thereof, wherein R1 represents the characterising chain of a saturated or unsaturated, straight or branched fatty acid comprising between 3 and 30 carbon atoms, R2 represents the characterising chain of an amino acid, R3 represents a hydrogen atom or a methyl radical or R3 combined with R2 and N constitutes the characterising chain of a cyclic amino acid, and m is between 1 and 50; between 0.1 and 20 mass % of magnesium and aluminium silicate; and up to 70 mass % of at least one topically acceptable ingredient. The invention also relates to the use of one such composition as a deodorising agent consisting of magnesium and aluminium silicate, in a topical cosmetic and/or pharmaceutical formulation comprising between 0.05 and 10 mass %, especially between 0.1 and 5 mass %, and preferably between 1 and 5 mass % of at least one compound of formula (I). The invention further relates to a method for reducing the odour caused by the presence of a compound of formula (I) in a topical cosmetic and/or pharmaceutical formulation, characterised in that magnesium and aluminium silicate are incorporated into said formulation.
CN101716168A Medicinal composition containing salt of desmethylvenlafaxine and method for preparing same The invention discloses a medicinal composition containing salt of desmethylvenlafaxine and a method for preparing the same. The medicinal composition consists of the salt of desmethylvenlafaxine and pharmacologically accepted auxiliary materials, and exists in a form of a gel tablet or wax tablet. The medicinal composition is mainly used for treating severe depressive disorder.
US20110178167 Method for inhibiting activity and/or expression of matrix metalloproteinase, inhibiting phosphorylation of mitogen-activated protein kinase, and/or promoting expression of collagen using terminalia catappa leaf extract A method for inhibiting the activity of matrix metalloproteinase (MMP), inhibiting the expression of matrix metalloproteinase, inhibiting the phosphorylation of mitogen-activated protein kinase (MAPK), and/or promoting the expression of collagen in a mammal is provided, and the method comprises administrating an effective amount of a Terminalia catappa leaf extract to the mammal.
US7871996 Contacting nitric oxide synthase with a corrin derivative; binding nitric oxide synthase but not nitric oxide; inflammatory, neurological disease, conjunctivitis, cystitis, inflammatory bowel disease, nephritis, glomerulonephritis, hepatitis, arteritis, vasculitis, cerebritis, vaginitis The present invention provides methods of inhibiting nitric oxide synthase (NOS) using corrin derivatives that bind NOS but do not bind NO. It also provides methods of inhibiting NOS in vivo by administering corrin derivatives, and methods of treating diseases and medical conditions using this inhibition of NOS.
CN103689748A Instant drink capable of regulating gastrointestinal function and preventing constipation The invention discloses an instant drink capable of regulating gastrointestinal function and preventing constipation. The instant drink consists of the following ingredients in parts by weight: 100-200 parts of sea buckthorn fruit powder, 5-100 parts of Chinese yam powder, 20-60 parts of fructus zizyphi sativae, 10-50 parts of honey, 1-50 parts of xylooligosaccharide and 5-60 parts of corn soluble dietary fiber. The product provided by the invention has the advantages of natural raw materials, unique formula and material selection, and reasonable and scientific production technology. Compared with other similar products, the product has a greatest characteristic that all raw materials belong to natural vegetables and fruits, thus the invention provides the functional food with obvious effect, no toxic and side effect and natural taste for day and night increased patients suffering from intestinal disorders and different degrees of constipation in current society.
CN101422450B Cajanus cajan L. natural medicine with blood sugar reduction and weight reduction function The invention discloses a natural medicament with the functions of hyperglycemic and lipid lowering as well as weight losing. The medicament is a resveratrol compound pigeon bean acid ketone A which can be prepared into a medicament preparation for curing diabetes or adiposity, and can also be prepared into a health-care food which is beneficial to a diabetes suffer or an adiposity suffer. The invention simultaneously discloses a compound of a plant source containing the pigeon bean acid ketone A as well as the use of the medicament and the health-care food thereof used for curing the diabetes.
CN102119924B Monodisperse nano aztreonam liposome preparation and preparation method thereof The invention belongs to the fields of medicament synthesis and preparations thereof, and relates to a stable aztreonam composition preparation and a preparation method thereof. A monodisperse nano aztreonam liposome preparation is prepared by adopting a membrane emulsifying technology. The method comprises the following steps of: suspending sterile beta-aztreonam in water for injection, and adding sterile L-arginine to regulate the PH value and dissolve all the beta-aztreonam to form a continuous phase; dissolving antioxidant-containing phospholipid for injection and cholesterol into ethanol to form a disperse phase; and dispersing the disperse phase into the continuous phase through a porous plasma membrane under the action of pressure, reducing the pressure to remove the ethanol, and performing sterilization, packing and freeze drying to obtain monodisperse nano aztreonam liposome for injection. The prepared particles have uniform size, high entrapment rate and good stability; the energy consumption is low and the conditions are mild in the emulsifying process, the reproducibility is better, the stability of an aztreonam medicament is increased, the toxic or side effect is reduced, and the availability of the medicament is improved; and the preparation method is simple in process and suitable for industrialized production.
US20080107639 Secreted glycoprotein for use in prevention and treatment of obesity, diabetes, osteoarthritis, liver and hypertensive disorders The present invention discloses novel uses for energy homeostasis regulating proteins and polynucleotides encoding this in the diagnosis, study, prevention, and treatment of metabolic diseases and disorders.
CN1899334A Treating agent for tooth ache The present invention discloses toothache treating medicine compounded with snake slough powder, ledebouriella root powder and glucose powder. The toothache treating medicine may be used in treating toothache caused by decayed tooth, pulpitis, gingivitis, maxillary sinusitis, etc.
EP1924592A2 Process for the synthesis of rocuronium bromide The invention encompasses processes for synthesizing l-[17β-acetyloxy-3α- hydroxy-2β-(4-morpholmyl)-5α-androstan-16β-yl]-l-(2-propenyl)pyrrolidinium bromide (rocuronium bromide) and intermediates thereof.
US8614190 Thermal responsive composition for treating bone diseases Thermal responsive compositions for treating bone diseases are provided. The thermal responsive composition for treating bone diseases includes a bone growth factor and a biodegradable copolymer. The biodegradable copolymer has a structure of Formula (I) or Formula (II): A-B-BOX-B-A Formula (I) B-A-B-(BOX-B-A-B)n-BOX-B-A-B Formula (II) wherein, A includes a hydrophilic polyethylene glycol polymer, B includes a hydrophobic polyester polymer, BOX is a bifunctional group monomer of 2, 2′-Bis(2-oxazoline) and used for coupling the blocks A-B or B-A-B, and n is an integer and the same or more than 0.
WO2008049402A2 Nail varnish remover for cosmetic and medical applications The invention relates to a nail varnish remover having improved nail care properties, that protects the nails from drying out and becoming brittle, promotes nail regeneration, positively influences the moisture content of the nail and gently removes a medical nail varnish from nails that are diseased or a cosmetic nail varnish from healthy nails. Said claimed nail varnish remover contains urea, dexpanthenol, a solvent and at least one oil having a weight proportion of more than 20% in wt. of fatty acids containing 10 - 25 carbon atoms, optionally together with additional conventional components such as keratolytic agents, permeation promoters, antioxidants, dyes, fragrances, conservation agents, skin-protective oils, antiseptics and similar.
CN102600152A Eutectic of dapoxetine and nicotinamide The invention relates to a eutectic of dapoxetine and nicotinamide, wherein the eutectic is formed by combining dapoxetine and nicotinamide. The eutectic of dapoxetine and nicotinamide disclosed by the invention is different from dapoxetine in X-ray powder diffraction and fusion point, so that the crystal morphology of the eutectic of dapoxetine and nicotinamide is completely different from that of dapoxetine in the prior art.
CN102018857B Externally applied medicament for treating chronic rhinitis The invention relates to an externally applied medicament for treating chronic rhinitis. The externally applied medicament for treating chronic rhinitis is prepared from the following raw materials in part by weight: 1 to 3 parts of pedate pinallia jackinthepulpit rhizome, 1 to 3 parts of Dutchmanspipe fruit, 2 to 4 parts of cortex dictamni, 2 to 4 parts of airpotato yam rhizome, 1 to 3 parts of red ochre, 3 to 5 parts of apocynum venetum, 3 to 5 parts of Himalayan teasel root, 2 to 4 parts of south dodder seed, 2 to 5 parts of moutan bark, 2 to 5 parts of Chinese angelica, 3 to 5 parts of tribulus terrestris, 3 to 5 parts of golden thread, 3 to 5 parts of weeping forsythiae, 4 to 6 parts of angelica dahurica, 1 to 3 parts of biond magnolia flower and 3 to 5 parts of Siberian cocklour fruit. The externally applied medicament for treating chronic rhinitis has the advantages of simplicity and convenience for use, small side effect, no irritant to skin, remarkable curative effect, quick response, reliable safety and convenience for popularization and use. The medicament has the effects of easing joint movement and dredging orifices, removing rot and regenerating muscle and clearing heat and releasing toxin, and can effectively treat various kinds of chronic rhinitis without performing an operation or puncturing. The total effective rate of the medicament reaches 100 percent.
CN103599075A Sustained release microspheres of polyethylene glycol-polylactic acid entrapped betamethasone dipropionate and preparation method thereof The invention relates to sustained release microspheres of polyethylene glycol-polylactic acid entrapped betamethasone dipropionate and a preparation method thereof. The sustained release microspheres are prepared from degradable high-molecular biomaterial polyethylene glycol-polylactic acid entrapped betamethasone dipropionate by an O/W type emulsification-solvent evaporation process, and are used for treating inflammatory diseases. The sustained release microspheres of polyethylene glycol-polylactic acid entrapped betamethasone dipropionate, provided by the invention, can regulate the release of a drug, prolong the action time of the drug, reduce the administration times, reduce the side effects of the drug and improve the drug effect. The preparation method provided by the invention is simple and reliable, can guarantee the product quality and application effect, and facilitates industrial production.
WO2010015794A1 Novel polymorphic forms of tegaserod The present invention relates to novel crystalline forms of tegaserod base and to processes tor the preparation of these novel crystalline forms. The invention also relates to pharmaceutical compositions comprising these, novel crystalline forms and to uses of said compositions in the treatment of patients suffering from gastrointestinal disorders. Formula (I)
CA2819859A1 Methods for treating baldness and promoting hair growth The invention relates to methods of treating baldness, treating alopecia, promoting hair growth, and/or promoting hair follicle development and/or activation or stimulation on an area of the skin of a subject (for example, a human) by subjecting said area of the skin to integumental perturbation. Integumental perturbation can be used in combination with other treatments for promoting hair growth. The invention provides devices for integumental perturbation for promoting hair growth, and provides pharmaceutical compositions for use in combination with integumental perturbation for promoting hair growth.
US20100113453 Sublingual Formulations of D-Cycloserine and Methods of Using Same The invention provides methods and compositions for treating anxiety-related disorders in a subject. The methods include sublingually administering D-cycloserine to a subject with the anxiety-related disorder, either alone or in combination with extinction training.
CN101797298B Ointment for treating eczema and preparation method thereof The invention relates to an ointment for treating eczema, which is prepared from the following raw materials of dyer woad leaf, red paeonia, plantain, forsythia, rhubarb, glauber salt, dittany bark, borneol, phellodendron, pepper, frutus cnidii and radix sophorae flavescentis. The invention also relates to a preparation method of the ointment. The ointment has reasonable formula and accurate curative effect and can effectively treat the eczema.
US20090013998 Inhalable tiotropium and container therefor A medical product suitable for storing and delivering a pre-metered dose of tiotropium, devices containing the same, and methods of using the same.
CN101361772A Oral medicine for treating traumatic injury and production method thereof The invention relates to an oral drug for traumatic injuries and a production method thereof (No.2 tablets for bone setting). The production method comprises the following steps: (1) various raw materials are selected according to mass portion as follows: 300 to 500 of angelica, 100 to 200 of ground beetle, 500 to 600 of membranaceous beautyleaf root, 100 to 200 of native copper and 500 to 600 of himalaya teasel; (2) 266 mass portions of the himalaya teasel is ground into fine powder (a sieve with a size of 5 and 80 meshes ) for a standby purpose; (3) the angelica, the ground beetle, the membranaceous beautyleaf root and the rest himalaya teasel that is not ground are added with water for decocting; the native copper is decocted individually; then two decoction liquids are combined and subjected to decompression-concentration for being prepared into a thick paste with a relative density of 1.35 to 1.40 (at 50 DEG C); (4) the standby fine powder of the himalaya teasel is added in the thick paste, evenly stirred, dried, ground, added with proper amount of alcohol (with a concentration of 70 percent to 80 percent) for pelletization, added with proper amount of accessories and then pressed into tablets. The drug for traumatic injuries has remarkable and stable treatment effects on various traumatic injuries, especially on fracture in early period, is convenient for taking, does not cause skin allergy or other untoward effects and has simple production technique, and finished products has stable quality and low price.
CN102861017A Application of compound on prevention and treatment of senile dementia The invention discloses an application of a compound on prevention and treatment of senile dementia and relates to a new application of a medicine, more especially, relates to application of the compound on prevention and treatment of senile dementia. The invention provides the application of the compound on prevention and treatment of senile dementia. The compound is 3-hydroxy-1, 2-dimethylpyridin-4(1H)-one), which can be utilized for preventing and treating the senile dementia as the medicine.
EP1863470B1 A method for preventing and/or treating vaginal and vulval infections The invention provides a method for treating and/or preventing a wide scope of vaginal and vulval infections, such as those caused by bacteria, parasites or yeasts, by administering gallic acid to a subject in need of treatment. A composition containing gallic acid for treating vaginal infections is also disclosed. It has been found that gallic acid is capable of selectively inhibiting the growth of Trichomonas vaginalis, a parasite that causes trichomonas vaginitis; Gardnerella vaginalis, a bacterium that causes bacterial vaginosis; and Candida albicans, a yeast that causes candidiasis and vulvitis; while not inhibiting the growth of Lactobacillus acidophilus, the dominant bacteria in a healthy vaginal ecosystem. Gallic acid is safe and cost-effective, and can be used alone or incorporated into different vaginal health products to treat and/or prevent vaginal infections.
WO2004035611A3 Peptides binding the phosphatase 2a protein and polynucleotides encoding same The invention concerns novel synthetic or natural E4orf4 or Bcl-2 peptides useful in particular in antitumoral, antiviral and antiparasitic treatments, said peptides having dimensions less than 33 amino acids and characterized in that they bind in vitro a phosphatase 2A protein holoenzyme or one of its subunits. The invention also concerns polynucleotides encoding the novel peptides, vectors expressing same, as well as antibodies identifying same and probes identifying transcripts thereof.
WO2008001859A1 OPIOID δ RECEPTOR AGONIST Disclosed are a compound represented by the formula (I) below and a pharmaceutical composition containing the compound. (In the formula, AA represents BB, CC or DD, and R1a, R1b, R2-R8, X and Y are as defined in the description.)
WO2005089775A1 Treatment and prevention of enterotoxigenic escherichia coli diarrhoeas A method of neturalising LT toxin produced by ETEC bacteria with a receptor mimic chosen from the group consisting of Galß[1→4]Glc-, Galβ [1→4]GlcNAcβ [1→3]Galβ[1→4]Glc-, and GalNAcβ [1→>4](NeuSAcα[2→3])Galβ[1→4]Glcβ-. ETEC bacteria are common in travellers diarrhea and thus the method is useful particularly as a preventative measure for travellers intending to go to destinations in which diarrhea is common. Similarly ETEC bacteria are a common cause of scours, particularly in weanling piglets and calves. The receptor mimics can be incorporated into drinking water or feed for these animals.
CN102973513A Intelligent nano-medicament delivery system and preparation method and application thereof The invention relates to an intelligent nano-medicament delivery system with pH responsiveness and a preparation method and application thereof. The delivery system comprises a nano-medicament carrier and a medicament encapsulated in the carrier, wherein the carrier is formed by a dendritic polymer and a molecular ligand connected to the carrier; the dendritic polymer is a polyamide-imide dendritic polymer or a polyamide-imide dendritic polymer containing cholate acid terminal group; and the molecular ligand is citraconic acid or 3, 4, 5, 6-tetrahydro benzoic acid. The medicament is an anti-tumor medicament or an induced differentiation medicament. The medicament delivery system is prepared by modifying a lower-generation polyamide-imide dendritic polymer, and the preparation process is simple. An experiment proves that the system plays a good cell delivery role on the anti-tumor medicament or a tumor differentiation medicament. The effect of the anti-tumor medicament can be effectively improved, the induced differentiation capability of an anti-differentiation medicament on cancer cells is improved, the toxic and side effect in an organism is small and the system can be used for treating cancers.
WO2009035020A1 Novel dihydronaphthalene compound and use thereof Disclosed is a compound represented by the formula (I) below as a dihydronaphthalene compound having a chemical structure which is excellent in production efficiency when compared with lasofoxifene and nafoxidine. This compound is useful as a proteasome inhibitor and/or an antitumor agent. (In the formula, two -(CH2)l-N(R1)(R2) groups represent a same substituent; R1 and R2 each represents a hydrogen atom, or a same or different alkyl group; or alternatively, R1 and R2 may combine together to form a monocyclic heterocyclic ring with a nitrogen atom having them or additionally together with one or more atoms selected from an oxygen atom, a sulfur atom and a nitrogen atom; R3, R4 and R5 each represents one or more substituents selected from a hydrogen atom, an alkyl group, an acyl group, an alicyclic group, an aromatic group, a halogen atom, an acyloxy group, a cyano group and a nitro group; l represents an integer of 2-5; n represents an integer of 1-4; m represents an integer of 1-5; and q represents an integer of 1-3.)
WO2011114246A1 Process for the preparation of malic acid salt of sunitinib The present invention relates to a process of preparation of malic acid salt of sunitinib.(I).
WO2007118717A2 METHOD FOR PREPARING 4-[17β-METHOXY-17α-METHOXYMETHYL-3-OXOESTRA-4,9-DIEN-11β-YL]BENZALDEHYDE (E)-OXIME (ASOPRISNIL) The present invention relates to a method for the reliable and reproducible preparation of 4-[17β-methoxy-17α-methoxymethyl-3-oxoestra-4,9-dien-llβ- yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).
CN102351846B Novel omeprazole sodium compound and medicinal composition thereof The invention discloses a novel omeprazole sodium compound. Characteristic peaks of the omeprazole sodium compound in an X-ray powder diffraction pattern obtained through Cu-K alpha-ray measurement are displayed when 2 theta is 3.2, 5.9, 7.6, 9.2, 10.5, 10.6, 12.3, 16.2, 18.2, 20.8, 23.4, 27.1, 30.4, 32.3 and 34.6. The omeprazole sodium compound has a new crystal form different from the prior art, has the thermodynamic stability higher than that with known crystal form, and has the advantage of not absorbing moisture basically. The invention also discloses a medicinal composition, which comprises the novel omeprazole sodium compound. Omeprazole sodium freeze-dried powder injection can be directly prepared under the condition of not adding lyoprotectants, and the omeprazole sodium freeze-dried powder injection has the advantages of high stability and high re-dissolubility.
WO2007057775A1 Spiropiperidine derivatives The invention provides compounds of formula (I): wherein the dotted line represents an optional covalent bond between X and Y, and X, Y, Z, m, R2, R3, R4, R5, R6, R7, R8, R9, a and b have the meanings given in the specification, and pharmaceutically acceptable salts and solvates thereof. The compounds are delta opioid receptor agonists and have a number of therapeutic applications, particularly in the treatment of pain.
CN101342163A Instant gel rubber of levobunolol hcl for eyes The invention discloses immediate type ophthalmic gelatin of hydrochloric acid levobunolol and a preparation method thereof. 100 milliliters of the immediate type ophthalmic gelatin of hydrochloric acid levobunolol contains 1 to 10 grams of the hydrochloric acid levobunolol, 0.05 to 1 grams of preservative, 1.0 to 7.5 grams of permeation pressure conditioning agent and 30 to 150 grams of gelatin substrate. Remaining components are acid-base buffer regent and water for injection. The invention enriches the dosage forms of the hydrochloric acid levobunolol by optimizing auxiliary materials and improving technology so that lag time in eyes is greatly prolonged and curative effect is improved without adverse stimulus reaction.
CN101116662A Application of sophocarpine in the preparation of medicine for treating adenovirus-caused inflammation The invention discloses the use of sophocarpine or the medicinal salt of sophocarpine in preparing medicine used to cure myocarditis and pulmonary inflammation caused by adenovirus, wherein the medicinal salt of sophocarpine is bromate, hydrochloride or fluorate of sophocarpine; the dosage form of the medicine can be of any dosage from recognized medically. The sophocarpine or the medicinal salt of sophocarpine has antibacterial action against adenovirus.
CN102614107A Micro-emulsion thermosensitive gel for skin external use and preparation method thereof The invention relates to the technical field of medicines, and in particular relates to a micro-emulsion thermosensitive gel for skin wound healing and a preparation method thereof. The micro-emulsion thermosensitive gel disclosed by the invention is composed of medicines, oil phase, a surfactant, a cosurfactant, a gel matrix and water, wherein the medicines are selected from resveratrol, paeonol and matrine. Proved by animal experiments, the prepared micro-emulsion thermosensitive gel has the characteristics of nearly no irritation to skin, safety in use, large percutaneous infiltration quantity, high percutaneous infiltration rate, long retention time of the micro-emulsion gel in the skin, high medicine concentration in the skin, good slow-release effect and good effect of promoting the healing of skin wound injury. The micro-emulsion thermosensitive gel disclosed by the invention has the advantages of simpleness in preparation method, low cost, convenience and safety in use and capability of effectively promoting the skin wound healing. According to the invention, a novel dosage form is provided for treating the skin wound.
US7223756 Treatment of autoimmune diseases, transplant rejection and rheumatoid arthritis with a quinazoline 4-substituted by a methylenedioxyphenyl group linked to the ring by an ether, methyl, sulfide, sulfoxide or sulfone, e.g., 6-methoxy-4-(2,3-methylenedioxyphenoxy)-7-(3-pyrrolidin-1-ylpropoxy)quinazoline, The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of m, R1, Z, n and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal
US20100240745 Method of treatment of inflammation in hypertensive patients The present invention relates to the use of 4-(nitrooxy)-butyl-(S)-2-(6-methoxy-2-naphthyl)-propanoate (naproxcinod) for the treatment of pain and/or inflammation in patients with hypertension treated with renin-angiotensin system blocking agents.
US20080069904 Inhibition of angiogenesis through nitric oxide tachyphylaxis A method is provided for treating cancer in a mammalian subject by inhibiting angiogenesis through the administration to the subject of a therapeutically effective amount of a nitrate-containing compound and a therapeutically effective amount of an inorganic selenium-containing compound. Kits and systems are also disclosed for practicing the subject methods.
US7208523 Slight toxicity and can be administered orally or intravenously to improve liver function The therapeutic agent for hepatitis, containing alanine and glycine, has only a slight toxicity and it can be administered either orally or intravenously to improve the liver function.
US20100160254 Cellulose Sulfate for the Treatment of Rhinovirus Infection The present invention provides the use of a polymer for the manufacture of an antiviral pharmaceutical composition for the treatment of a rhinovirus infection, wherein the polymer is cellulose sulfate.
CN101444486B Water-soluble drug sustained-release microsphere and preparation method and applications thereof The invention discloses a water-soluble drug sustained-release microsphere and a preparation method and applications thereof. The microsphere comprises an inner core area and an outer core dispersing area; the inner core area is formed by using an isolating oil phase to seal the water-soluble drug; the outer core dispersing area is a medical macromolecular accessory. The invention discloses the preparation method for the water-soluble drug sustained-release microsphere; the medical macromolecular accessory is dissolved into an organic solvent to form a dispersing medium; the powder of the water-soluble drug is dispersed into an isolating layer oil phase to form suspension liquid and slowly release into the dispersing medium; then the suspension liquid is prepared into first milk; then thefirst milk is prepared into emulsion. The organic solvent is volatilized to form the microsphere; the suspension liquid dispersed with the microsphere is centrifugated, filtered, washed, dried and collected, thus obtaining the microsphere. The invention also discloses an emulsion-solvent vaporizing method to prepare the water-soluble drug sustained-release microsphere and the applications of the preparation method in different drug preparations. The microsphere preparation technique is stable, and practical; the shape of the microsphere is round; the surface is smooth, the fluidity is good and the granularity distribution is uniform.
US20060004077 Inhibiting class II MHC-mediated activation of T cells; peptidomimetics of given sequence which include a Gpg (guanylpiperidyl glycine) unit; rheumatoid arthritis and/or multiple sclerosis; e.g. Ac-Cha-Gpg-Tic-Nle-NHCH2CH2Ph (Cha=cyclohexylalanine, Tic=3-carboxyisoquinoline, Nle=norleucine) The present invention relates to compositions and methods for suppressing an immune response, e.g., by inhibiting class II MHC-mediated activation of T cells. The subject compounds and methods may be used to treat or prevent disorders such as rheumatoid arthritis and/or multiple sclerosis.
US20120321563 Carbonic Anhydrase Targeting Agents and Methods of Using Same The invention provides agents that target carbonic anhydrase, which can be used as imaging agents or therapeutic agents. The agents can be used to image tumor hypoxia as well as other physiological processes in a subject.
US7291611 Including indanones, indolinones and benzoxazolinones containing a piperidine ring, e.g., 1-[3-(4-(Hydroxymethyl)piperidin-1-yl)propyl]-1,3-dihydrobenzoimidazol-2-one; particularly for the M1 and/or M4 receptor subtypes; increase acetylcholine signaling or effect in the brain Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
US20080069901 Using cisplatin; therapy for bone or liver cancer; oral bioavailable To provide a therapeutic agent for metastatic cancer and a cancer metastasis inhibitor which are highly safe and efficaciously treat metastatic cancer and inhibit cancer metastasis, and especially efficaciously treat and inhibit cancer metastasis to bone and liver. There are provided a therapeutic agent for metastatic cancer and a cancer metastasis inhibitor each of which includes a platinum complex having an anticancer activity as an active ingredient. The platinum complex is preferably cisplatin. The therapeutic agent for metastatic cancer is advantageously usable for treating metastatic cancer to bone and/or liver. The cancer metastasis inhibitor is advantageously usable as a cancer metastasis inhibitor for inhibiting metastasis to bone and/or liver. These agents can advantageously further include a bisphosphonate as another active ingredient.
WO2006137706A1 6-(4-substituted-anilino)pyrimidine derivatives, method for preparing thereof and antiviral pharmaceutical composition comprising the same 6-(4-substituted-anilino)pyrimidine derivatives represented by Formula 1 having an excellent inhibitory effect on replication of Hepatitis C virus (HCV) or pharmaceutically acceptable salts thereof, a method for preparing thereof and an antiviral pharmaceutical composition comprising the same. The novel 6-(4-substituted- anilino)pyrimidine derivatives represented by Formula 1 have an excellent inhibitory effect on replication of Hepatitis C virus (HCV) and low toxicity thus can be advantageously used as a therapeutic or prophylactic agent of hepatitis C.
CN101732344A Preparation for treating alcohol positive milk of dairy cow The invention discloses a preparation for treating alcohol positive milk of a dairy cow and provides an oral preparation for treating the alcohol positive milk of the dairy cow for dairy cow farmers. The preparation comprises the following main components in part by weight: sodium citrate, potassium iodide, sodium dihydrogen phosphate and medical stones. The formulation of the preparation is powder. The preparation has the effects of regulating metabolic functions of mammary glandular cells, improving milking capacity of the mammary glandular cells, promoting milk colloidal state to be balanced and stable and the like. Four-year clinical practice and research prove that the preparation has the advantages of reliable curative effect, convenient use, safety and no side effects.
WO2008023784A1 Agent for amelioration of ophthalmic circulatory disorder Disclosed is an agent for ameliorating an ophthalmic circulatory disorder for orally administering limaprost to a patient with the ophthalmic circulatory disorder in an amount of 5 to 50 μg per day for a period of 2 to 72 weeks. The agent can be administered orally to ameliorate the ophthalmic circulatory disorder, and treat a symptom induced by the ophthalmic circulatory disorder and/or prevent the progress of the symptom. Further, the agent can shorten the period required for disappearance of the hemorrhage of the optic fundus associated with the ophthalmic circulatory disorder and also shorten the period required for the recovery of decreased visual acuity and/or the amelioration of a visual field disorder.
WO2006044573A3 Reversible inhibitors of s-adenosyl-l-homocysteine hydrolase and uses thereof The present invention provides compositions and methods for reversibly inhibiting Sadenosyl-L-homocysteine (SAH) hydrolase. The compounds of the present invention can be used in combination with an anti-hemorrhagic viral infection agent, an immunosuppressant, a homocysteine lowering agent, or an anti-neoplasm agent. The compositions and methods of the present invention can be used for the prevention and treatment of hemorrhagic virus infection, autoimmune diseases, autograft rejection, neoplasm, hyperhomocysteineuria, cardiovascular disease, stroke, Alzheimer's disease, or diabetes.
CN101940598B Preparation method of Huang children paracetamol-particles The invention relates to a preparation method of Huang children paracetamol-particles. The Huang children paracetamol-particles are prepared from the following raw materials in percentage by weight: 1.8-2.2% of paracetamol, 0.08-0.1% of Calculus Bovis Artifactus, 0.008-0.01% of chlorpheniramine maleate and 95-99% of other auxiliary material; and the auxiliary material comprises one or more of sucrose, steviosin, soluble saccharin, aspartame, vanillin, strawberry essence, tangerine essence and the like. The materials are mixed, and slushed with purified water and chlorpheniramine maleate as wetting agent. The preparation method comprises the following steps: (1) mixing and pulverizing part of sweetening agents and Calculus Bovis Artifactus, pulverizing and adding the rest of sweetening agents in an equally progressive increase mode, and mixing the mixture and pulverized paracetamol in a trough type mixing machine; (2) mixing with the wetting agent to prepare soft material, screening toobtain particles; and (3) fluidized-drying, adding essence particles, totally mixing, testing to obtain a qualified product, packaging into small bags, and packaging into exterior bags. The inventionhas the advantages of favorable content uniformity, high bioavailability and low production cost.
WO2005067906A3 Pharmaceutical composition comprising 2,4-dichlorobenzyl alcohol and amylmetacresol A pharmaceutical composition comprising 2,4-dichlorobenzyl alcohol in combination with amylmetacresol for the treatment or prevention of viral infections caused by SARS-associated coronavirus.
US20120003184 Sodium salt of 5-cyclopropyl-2-benzoic acid as dhodh inhibitor The present disclosure is directed to the sodium salt of 5-cyclopropyl-2-{[2-(2,6-difluorophenyl)pyrimidin-5-yl]amino}benzoic acid, pharmaceutically acceptable solvates thereof, pharmaceutical combinations thereof, and methods of treatment.
CN101897776A New application of Chinese flowing crabapple extractive and phlorizin The invention provides a new application of Chinese flowing crabapple extractive and phlorizin, in particular relating to an application in preparing a drug or a health care food for adjusting estrogen. The Chinese flowing crabapple extractive and phlorizin in the invention has the function of adjusting the estrogen in a two-way manner, definite potency and strong controllability, and provides a new choice for clinic drugs or health care foods.
CN103641841A Sesquiterpene lactone compounds as well as preparation method and application thereof The invention provides a sesquiterpene lactone compound as well as a preparation method and application thereof, wherein the compound has a structure shown in a structural formula (I) or (II). The sesquiterpene lactone compound provided by the invention can be used as a drug for treating cachexia of human and animals, and is capable of treating the cachexia associated with various diseases. The sesquiterpene lactone compound is capable of effectively slowing down the loss of weight caused by skeletal muscle atrophy and fat degradation atrophy, obviously reducing tumor load, inhibiting the degradation of protein and increasing the levels of cell factors TNF-A and IL-6.
US20070031344 Aerosolized anti-infectives, anti-inflammatories, and decongestants for the treatment of sinusitis Pharmaceutical compositions are described that contain one agent for treatment of sinusitis and a surfactant. The compositions are prepared to have a surface tension that renders the composition effective for treatment of sinusitis.
US20070243270 prevent skin damage caused by ultraviolet radiation by administering a oral dosage of alpha-lipoic acid, n-acetyl cysteine, green tea extract, turmeric extract, and quercetin, and applying s topical dosage form comprising plant extracts of berry, bitter orange peel, lemon, cucumber and herbs Methods of reducing cellular damage are described that include (a) administering to the mammal an oral dosage form comprising a therapeutically effective amount of a first antioxidant, and (b) administering to the mammal a topical dosage form comprising a therapeutically effective amount of a second antioxidant, wherein at least one of the first antioxidant and the second antioxidant comprises acerola concentrate. Methods of inhibiting free radical production, methods of scavenging free radicals, and kits for reducing cellular damage are also described.
CN103006704A Manufacture method of sodium phosphate medicament The invention discloses a manufacture method of a sodium phosphate medicament. The method comprises the following steps of 1, component weighing: weighing sodium dihydrogen phosphate monohydrate, sodium phosphate dibasic heptahydrate, glycerol, saccharin sodium, sodium benzoate, ginger essence and lemon essence in a weight ratio of 480g:180g:15g:3.3g:0.35g:0.5ml, and delivering to the next step; 2, preparing: adding purified water into saccharin sodium and sodium benzoate for the first time, heating to boiling, stirring to dissolve the saccharin sodium and sodium benzoate; adding disodium hydrogen phosphate and sodium dihydrogen phosphate, heating and stirring until disodium hydrogen phosphate and sodium dihydrogen phosphate are completely dissolved, standing to lead the mixture is cooled to 60 DEG C; weighing glycerol in the amount of the prescription, adding the ginger essence and the lemon essence, stirring to dissolve, adding the mixture of essence and glycerol into the liquid, stirring to dissolve the essence and the glycerol, adding the purified water for the second time to a preset amount, and uniformly stirring; and measuring the content, and filtering. The method has the advantages that the sodium phosphate medicament with excellent quality can be produced.
US8288407 Substituted naphthyridine compounds as inhibitors of Akt activity The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. Compounds disclosed herein have the following chemical structure:
US20070112002 1-[2-(4,4-dimethylcyclohexyl)-5-methoxyphenyl]-4-pentylpiperazine; excellent cell adhesion inhibitory action or cell infiltration inhibitory action; inflammatory diseases and autoimmune diseases such as ulcerative colitis, Crohn's disease, irritable bowel syndrome, rheumatoid arthritis, psoriasis, asthma A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.
CA2313024C Pharmaceutical compositions containing an omega-3 fatty acid oil Self-emulsifying microemulsion or emulsion preconcentrate pharmaceutical compositions containing an omega-3 fatty acid oil such as a fish oil and a poorly water soluble therapeutic agent such as cyclosporin are formulated for administration, particularly oral administration to a human. The preconcentrates, which are substantially free of or contain only minor amounts of a hydrophilic solvent system, contain a pharmaceutically effective amount of an omega-3 fatty acid oil; a therapeutically effective amount of a poorly water soluble therapeutic agent that is substantially soluble in the omega-3 fatty acid oil; and a surfactant system comprising at least one surfactant. Microemulsions or emulsions formed by diluting the self-emulsifying preconcentrate with an aqueous solution are also provided.
CA2129046C Opioid diarylmethylpiperazines and piperidines Diarylmethyl piperazine/piperidine compounds of formula (1) as shown above wherein the substituents are as defined in the description having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/ or kappa receptors. Compounds of the invention may be employed as conjugates in agonist/antagonist pairs for transductional monitoring and assays of neurotransmitter function, and also variously exhibit therapeutic utility, including mediating analgesia, and possessing utility for the treatment of diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depression, asthma, emphysema, and apnea, cognitive disorders, and gastrointestinal disorders.
WO2006097730A1 Analogues of the azinomycins as anti-tumour agents and as prodrugs Compounds of general formula (I) or a salt thereof in which R1 is preferably an aromatic DNA binding subunit are oxidation- activated prodrugs. The compounds are expected to be converted into an epoxide at the alkene to which R2 is attached by cytochrome P450, in particular CYPIBI, expressed at high levels in tumours. R3 preferably comprises a Nitrogen mustard to provide a prodrug which has 2 alkylating groups. The prodrugs are expected to be activated preferentially in tumour cells.
CN101744811A Bulleyaconitine A and adrenaline compounded sterile powder for injection The invention relates to bulleyaconitine A and adrenaline compounded sterile powder for injection, belonging to a medicinal preparation containing effective organic components, in particular to a medicinal preparation containing bulleyaconitine A. The bulleyaconitine A and adrenaline compounded sterile powder for injection is prepared by adding 1-2 micrograms of adrenaline sterile powder for injection to 0.1-0.3 milligram of bulleyaconitine A sterile powder for injection. Compared with a single bulleyaconitine A preparation, the bulleyaconitine A and adrenaline compounded sterile powder can more greatly reduce the side effects of flustration, nausea, palpitation, and the like on the respiratory system and the cardiovascular system, which is generated by the single bulleyaconitine A preparation, and achieves the therapeutic action of the bulleyaconitine A on easing chronic pains and anti-inflammation.
CN101724050A Human epididymal expression sperm binding protein HEL-214 as well as encoding gene and application thereof The invention belongs to the biotechnology and the medical field and discloses a new human epididymal specific expression sperm binding protein HEL-214 as well as preparation and application thereof. The invention discloses an amino acid sequence of the HEL-214 protein and provides a recombinant expression vector which carries a DNA sequence used for encoding the protein. The protein is located in a back region of the head of a mature sperm, has higher expression level in an epididymis, a testis and a liver and has lower expression level or no expression in other tissues. A band of about 15 KD is detected in the epididymis by using Western blot. The HEL-214 protein can be used as a target protein for developing an immunological contraceptive and clinically diagnosing and treating male infertility. A method for detecting a corresponding gene or protein based on development of the HEL-214 protein can be widely used for the research field of reproductive medicine.
CN1973902B Anticancer medicine adriamycin composition with ginseng polyse as carrier and its preparation process The present invention belongs to the field of pharmaceutical technology, and is especially antitumor medicine adriamycin composition with ginseng polysaccharide as carrier and its preparation process. The present invention adopts ginseng polysaccharide as the directional and slow releasing carrier for chemotherapeutic medicine adriamycin, and peptide chain comprising 3 or 4 amino acids as the connector between adriamycin and ginseng polysaccharide molecule. After the medicine reaches the pathological change part, the peptide chain is hydrolyzed by body's protease to release antitumor medicineadriamycin and ginseng polysaccharide while the peptide chain is degraded into non-toxic amino acids, so that adriamycin can act on the disease focus tissue concentratively to kill cancer cell and improve the body's immunologic function.
EP1399440B1 5-(2-aminopyrimidin-4-yl)benzisoxazoles as protein kinase inhibitors Described herein are benzisoxazole compounds of formula I or a pharmaceutically acceptable derivative or prodrug thereof, wherein A-B is N-O or O-N; Ar is an optionally substituted C5-10 aryl group; R1 is hydrogen or an optionally substituted group selected from C1-I0 aliphatic, C¿5-10? aryl, C6-12 aralkyl, C3-10 heterocyclyl, or C4-12 heterocyclylalkyl; and T, n, R?2 and R3¿ are as described in the specification. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3 and JAK mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various -, protein kinase mediated disorders.
CN102727465A Nicotine-containing patch preparation An object of the present invention is to provide a nicotine-containing patch preparation which enables to suppress degradation of nicotine and coloring of the patch preparation. The present invention provides a patch preparation comprising a support and an adhesive layer on its at least one surface, wherein the adhesive layer comprises an adhesive polymer, nicotine and a stabilizer, and the stabilizer is at least one kind selected from the group consisting of butylhydroxyanisole (BHA), propyl gallate (PGA), dibutylhydroxytoluene (BHT) and 2-mercaptobenzimidazole (MBT).
WO2014025679A1 Process for the preparation of c-fms kinase inhibitors The present invention is directed to a process for the preparation of heterocyclic derivatives of formula I (I), wherein J, X, Z, W and R2 are as defined herein using a palladium catalysed aminocarbonylation reaction. Such compounds are useful as protein tyrosine kinase inhibitors, more particularly inhibitors of c-fms kinase.
CA2281133C Multiple-agents-binding compound and use thereof The present invention is to provide a multiple-agents- binding compound comprising a compound having anti-HIV activity and having no affinity for cell surface protein bound together with a same or different kind of at least one compound having anti-HIV activity and having no affinity for cell surface protein, or a salt thereof, and a pharmaceutical composition for the prevention or treatment: of infectious disease of HIV or AIDS comprising said multiple-agents-binding compound.
US7365191 immunology; antitumor agents; viricides; anticancer agents; antiinflammatory agents; oligosaccharde containing glucose, galactose, mannose This invention involves a type of oligosacoharides and its their sulfate derivatives. The backbone of the oligosaccharides consists of 4 to 14 glucose residues, while the side chains contain 0 to 4 glucose residues. There are at least one 1->3α linkage and β-(1->3)-Iinkage or β-(1->4) linkage in the backbone. These oligosaccharides, and their sulfates have immune enhancing, antitumor, and antiviral activities. They can be used in immune enhancing, antitumor, and antiviral medicine compounds that would be used as therapeutic treatments.
CN101313948A Xianzi muscle promoting plaster The invention provides a Xianzi ointment for promoting tissue regeneration, relating to an external use medicine. The ointment is characterized by being prepared by the following materials in weight portion: 50 to 100 portions of sinkiang arnebia root, 50 to 100 portions of agrimony, 50 to 100 portions of rhubarb, 30 to 60 portions of bark of Japanese pagodatree, 5 to 10 portions of borneol, 500 to 1,000 portions of sesame oil and 100 to 300 portions of yellow wax. The preparation method comprises the following steps that: the materials are immersed in the sesame oil for 12 hours, boiled by slow fire, filtered and added with proper amount of yellow wax, and the ointment is prepared, and the whole preparation process is ensured to be free from bacteria. The Xianzi ointment for promoting tissue regeneration prepared by the method of the invention has the obvious advantages of good inflammation diminishing effect, quick tissue regeneration and no scar, etc.
CN1602858A Arteannuin preparation for treating gynecopathy The invention provides a preparation of arteannuin for curing gynecological diseases, which is made into a medical acceptable preparation by auxiliary materials and effective compound of medicine. Its characteristic is that its effective component is arteannuin or its derivativeand each smallest preparation unit contains effective preparation 0.02g-1.0g, it has remarkable inhibitory action or killing action to pathogen such as colpitis mycotica and trichomonad. besides, by adding organic acid like citric acid to adjust its pH value, its medical effect can also be played in the acid environment of focus, since aromatic can also be added, the medicine has better effect for eliminating wetness-evil with drugs of fragrant flavor, meanwhile, the fragrance radiating from the medicine is suitable for human design. The invention has remarkable inner quality, increasing sicker's aromatic and supplying basis for increasing curative effect or even eradicate disease.
US20110020443 Slow release magnesium composition and uses thereof The present invention provides compositions that contain magnesium and threonate, or a threonate precursor molecule, formulated for extended or modified release to provide physiological concentrations over a desired time period. The extended release or modified release form is particularly useful in providing Mg to a subject while avoiding adverse side effects such as diarrhea.
US20120302514 Glycoconjugates and methods Disclosed are compositions containing glycoconjugates and methods for making the functionalized glycoconjugates, which include (a) contacting a cell with a first monosaccharide, and (b) incubating the cell under conditions whereby the cell (i) internalizes the first monosaccharide, (ii) biochemically processes the first monosaccharide into a second saccharide, (iii) conjugates the saccharide to a carrier to form a glycoconjugate, and (iv) extracellularly expresses the glycoconjugate to form an extracellular glycoconjugate comprising a selectively reactive functional group. Methods for forming products at a cell further comprise contacting the functional group of the extracellularly expressed glycoconjugate with an agent that selectively reacts with the functional group to form a product. Subject compositions include cyto-compatible monosaccharides comprising a nitrogen or ether linked functional group selectively reactive at a cell surface and compositions and cells comprising such saccharides.
WO2010005384A1 Ketone pyridine analogues and their use in the treatment of cardiovascular disorders The present invention relates to certain new pyridin analogues of Formula ( I ) to processes for preparing such compounds, to their utility as P2Y 12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
US20120184566 Substituted dihydro benzocycloalkyloxymethyl oxazolopyrimidinones, preparation and use thereof The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I): Wherein n, R1, R2, R3, R4, R5 and R6 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
CN102101825A PTP1B (Protein Tyrosine Phosphatase 1B) inhibitor, and synthesis and application thereof The invention relates to a novel chemical complete synthesis method of a PTP1B (Protein Tyrosine Phosphatase 1B) inhibitor and application of the PTP1B inhibitor in medicaments for treating Type 2 diabetes. The chemical structural formula of the PTP1B inhibitor is disclosed in the specification, wherein groups connected to the 2-site, 2'-site and 3-site carbons of the benzene ring are bromine atoms; the 4-site, 4'-site, 5-site and 5'-site carbons are connected to hydroxyl groups; and the English chemical name of the compound is (2'-bromo-4',5'-dihydroxy-phenyl)-(2,3-dibromo-4,5-dihydroxy-phenyl)-methane. By inhibiting the activity of the protein tyrosine phosphatase 1B, the compound enhances the insulin receptor sensitivity, and has favorable therapeutic action on insulin resistance Type 2 diabetes.
US20080221198 Novel Crystalline Forms of Antidiabetic Compounds Novel crystalline forms of two indole compounds connected to phenoxyalkylcarboxylic acid groups are selective PPAR gamma partial agonists that are useful in the treatment of type 2 diabetes, hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. The novel crystal forms include a crystalline free acid dihydrate and crystalline free acid anhydrate of one compound and several crystalline forms of the free acid and the sodium salt of the second compound. The invention also relates to pharmaceutical compositions comprising these novel crystal forms, processes to prepare the crystal forms and their pharmaceutical compositions, and uses of the crystal forms in the treatment of type 2 diabetes and other PPAR gamma modulated diseases.
US8664222 Specific salt, anhydrous and crystalline form of a dihydropteridione derivative The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallization in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.
US20110250137 Radioisotope-labeled lysine and ornithine derivatives, their use and processes for their preparation The invention relates to the compounds suitable for radiolabeling with a chelator free radioisotope and radiolabeled compounds of the general Formula I. Said compounds are ornithine or lysine derivatives.
CN103127139A Difluprednate topical external preparation Difluprednate topical external preparation comprises difluprednate micro powder used as active ingredients and one type or multiple types of pharmaceutic adjuvants, wherein the pharmaceutic adjuvants comprise water. The difluprednate topical external preparation is characterized in that the difluprednate micro powder is scattered in the pharmaceutic adjuvants in a suspended mode, the difluprednate is difluprednate crystal form I, and the X-ray powder diffraction of the difluprednate crystal form I has a characteristic peak when a diffraction angle 2theta is 8.9 degrees, 11.6 degrees and 17.6 degrees.
US7022521 Methods and compositions for treating platelet-related disorders using MPL pathway inhibitory agents The invention relates to the treatment of subjects for the purpose inhibiting vaso-occlusive events, including thrombosis and embolism, by administering agents which reduce the number of circulating platelets to low or below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.
CN102028656A Cetirizine dihydrochloride spray Aiming at the defects of inconvenient use of a cetirizine dihydrochloride spray in treatment of body surface allergic diseases, and undesirable effects of the cetirizine dihydrochloride spray, ordinary liniments, liposome liniments on mosquito bite treatment, by optimizing a formula according to physicochemical properties of the cetirizine dihydrochloride, and screening more suitable auxiliary materials during the experiment, the invention provides a cetirizine dihydrochloride spray which is convenient in use and significant in effect on anti-allergic efficacy and mosquito bite treatment. Compared with previous cetirizine dihydrochloride sprays, the cetirizine dihydrochloride spray provided by the invention has the following advantages: simple preparation technology, lower cost, almost no skin irritation and wide application value.
EP1638555A1 Substituted 5-membered ring compounds and their use Compound of a compound of formula (I) or a salt, N-oxide, hydrate or solvate thereof, in the preparation of a composition for inhibition of HSP90 activity: wherein ring A is an aromatic or non-aromatic carbocyclic or heterocyclic ring having 5 ring atoms, for example 1,2,3-triazolyl or a 1,2,4-triazolyl or a tetrazolyl ring; and R1 R2 R3 are as defined in the specification are inhibitors of HSP90 and therefore of use in the treatment of, for example, cancers, viral disease, inflammatory diseases such as rheumatoid arthritis, asthma, multiple sclerosis, Type I diabetes, lupus, psoriasis and inflammatory bowel disease; cystic fibrosis angiogenesis-related disease such as diabetic retinopathy, haemangiomas, and endometriosis; or for protection of normal cells against chemotherapy-induced toxicity; or diseases where failure to undergo apoptosis is an underlying factor; or protection from hypoxia-ischemic injury due to elevation of Hsp70 in the heart and brain; scrapie /CJD, Huntingdon's and Alzheimer's disease.
CN101671293A Alpha-glycosidase inhibitor compound in silkworm excrement total alkaloid and application thereof The invention obtains (2R, 4R)-dihydroxy-5(R) hydroxymethyl piperidine (new compound) and 1-DNJ from silkworm excrement total alkaloid through separation. Enzymological measurement shows that the twoalkaloids have certain inhibitory activity to alpha-glycosidase. The alpha-glycosidase inhibitor compound can be applied in preparing machines for treating disasters such as diabetes, obesity and thelike.
CN1861042A Weiding ointment and its prepn. process A Weiding cream for treating allergic dermatitis, eczema, psoriasis, etc is proportionally prepared from efcorlin butyrate, VE and cream matrix. Its preparing process is also disclosed.
US20120121711 Microsphere drug carrier, preparation method, composition and use thereof A nanosphere or microsphere drug carrier, formulations comprising the drug carrier and the preparation method of the formulations and the use of the carrier are disclosed. The carrier comprises a biodegradable methoxy end-capped polyethylene glycol-polylactide block copolymersor a derivative thereof represented by formula (I) as the main carrier material: CH3O—[CH2—CH2—O]m—[C(O)—CH(CH3)—O]n—R (I).
WO2009001021A1 Imidazopyridine derivatives useful as enzyme inhibitors for the treatment of cell proliferative and autoimmune diseases The 62 specific compounds disclosed in the description, which fall within the general structural formula (I) below, are inhibitors of aurora kinase enzymes: wherein X is -N-, -CH2-N-, -CH2-CH-, or -CH-; R1 is a radical of formula (IA) wherein Z is -CH2-, -NH-, -O-, -S(O)- -S-, -S(O)2 or a divalent monocyclic carbocyclic or heterocyclic radical having 3-7 ring atoms; AIk is an optionally substituted divalent C1-C6 alkylene radical; A is hydrogen or an optionally substituted monocyclic carbocyclic or heterocyclic ring having 5-7 ring atoms; r, s and t are independently 0 or 1, provided that when A is hydrogen then at least one of r and s is 1; R2 is halogen, -CN, -CF3, -OCH3, or cyclopropyl; and R3 is a radical of formula (IB) wherein Q is hydrogen or an optionally substituted phenyl or monocyclic heterocyclic ring with 5 or 6 ring atoms; Z1 is -S-, -S(O)-, -S(O)2-, -O-, -SO2NH-, -NHSO2-, NHC(=O)NH, -NH(C=S)NH-, Or -N(R4)- wherein R4 is hydrogen, C1-C3 alkyl, cycloalkyl, or benzyl; and AIk1 and AIk2 are, independently, optionally substituted divalent C1-C3 alkylene radicals; and m, n and p are independently O or 1.
US20100035945 Small molecule inhibitors of bacterial dam dna methyltransferases Disclosed are compounds, crystal structures, data representations, methods of using, and methods of identifying compounds in relation to DNA methylation and inhibition of methylation. In embodiments, DNA methylation is by DNA-adenine methyltransferases (Dam). In an embodiment, compounds are used to treat a host suspected of infection by a pathogenic organism. In an embodiment, virulence of a pathogenic bacterium is modified by treatment with an agent capable of inhibiting a bacterial Dam enzyme. In an embodiment, compounds and methods are disclosed regarding Dam inhibitors.
CN101357939B Protein conjugate and pharmaceutical compositions thereof The invention discloses a novel protein conjugate which is the conjugate of proteins and endogenous substances modified by cystine or cysteine. Besides, the invention also discloses a drug combination comprising the protein conjugate and the preparation method of the protein conjugate and the drug combination comprising the protein conjugate. The invention does not relate to toxic organic solvents and catalysts, reactions are simple and easy, and products are easy for separation, refinement and quality control, and moreover, the active targeting property of the obtained drug combination is improved.
CN101066260B Coenzyme Q10 emulsion and its freeze dried emulsion and their preparation process The present invention discloses a novel pharmaceutical composition, coenzyme Q10 emulsion and freeze-dried emulsion, and a preparation method thereof. The emulsion comprises coenzyme Q10 as the medicinal component in 0.25 %, and medicinal supplementary material including oil phase 1-20 %, emulsifier 0.01-10 %, auxiliary emulsifier 0.001-5 %, stabilizer 0-2 % and isoosmotic regulator 1-10 % as the balance. The freeze-dried emulsion contains coenzyme Q10 in 0.25-1.0 %, a freeze-dryed protective agent and water for injection as the balance. According to the ingredients of the coenzyme Q10 emulsion, the freeze-dried emulsion and the preparation method thereof, the particle diameters of both the coenzyme q10 emulsion and the freeze-dried emulsion are less than 500 nm belonging to the category of sub-nanometer emulsions. The particle diameter of the freeze-dried emulsion is not changed significantly. Before use, the freeze-dried emulsion is reconstructed by adding water, wherein the freeze-dried emulsion is quickly re-dissolved to be renewed as a sub-nanometer emulsion. Meanwhile, no crystalline is precipitated during the dilution of the freeze-dried emulsion. The initial stability test shows that the pharmaceutical composition is better in stability and light stability, compared with common solution type preparations. The safety test shows that the pharmaceutical composition meets the safety requirement and can be used for clinical intravenous injection and oral administration.
EP1764134A2 Tetrahydroindolone and purine derivatives linked to arylpiperazines Pharmaceutical composite compositions comprising tetrahydroindolones linked to arylpiperazines and derivatives thereof are disclosed. Specifically, composite compositions useful in treating anti-psychotic disorders are disclosed. The composite compositions disclosed herein can effectively ameliorate symptoms and treat psychotic disorders without causing a decrease in cognitive function. Generally, the composite compounds consist of two moieties, moiety A and B in which a tetrahydroindolone comprises a moiety A linked through a linker L to a moiety B, where B is an arylpiperazinyl moiety. The composite compound provides anti-psychotic actively by interaction with GABA, seratoninne and dopamine receptors. The composite molecules with the combined activities will provide treat psychiatric and neurological diseases without cognitive impairment.
CN103479726A Medicament for treating chronic nasosinusitis and preparing method thereof The chronic nasosinusitis is a disease with nasal obstruction, pus snot flowing, dizziness, headaches and hyposmia as major expressions. The disease course is long and can be several years to tens of years, and the chronic nasosinusitis can repeatedly attack patients, prolong a long time and be difficult to heal. The chronic nasosinusitis is mostly caused by infections of bacteria in the paranasal sinus, and the pathogenic bacteria are mainly bacillus influenzas and streptococci. The chronic nasosinusitis is also called as sinusitis, the number of the patients suffering from the chronic nasosinusitis is large and is almost a half of that of rhinopathy patients, and most of the patients suffering from rhinopathy are suffering from chronic maxillary sinusitis. If lesions are caused on polyparanasal sinus on one side or the two sides, the patients are suffering from the polysinusitis or pansinusitis, and the chronic nasosinusitis generally occurs secondary to acute nasosinusitis. The chronic nasosinusitis has a close relation to paranasal sinus drainage blocking, weak human body resistance or strong germs, most of the patients do not have obvious constitutional symptoms, the patients generally have the symptoms of dizziness, doldrums, memory deterioration and the like and being easy to fatigue, the most common symptoms are nasal obstruction, pus flowing, snot flowing, poor smell and the like, and then the chronic nasosinusitis can be divided into the lung-cold type and the spleen-weak type. In the modern western medicine, except for puncturing, washing and operative treatments, no ideal treatment measure exists, and many chronic nasosinusitis patients cannot dare to be treated.
US7012089 Administering to a patient suffering from psychological disoders a (1,4)diazocino(7,7,1-hi)inodle derivative as 5HT2c agonist or partial agonist Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: where R1 through R7 are defined herein. The compounds of formula (I) are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
CN101283965B Preparation containing bendopa methyl ester and preparation method thereof The invention discloses a preparation containing L-dopa methyl ester and a preparation method thereof. The preparation method comprises the following steps of: adding L-dopa methyl ester into a meltedcarrier material such as polyethylene glycol (PEG), poloxamer 188 or hydroxypropyl cellulose (HPC), stirring at high speed to uniformly disperse drug particulates into the carrier material, making into solid dispersion, and further making into capsule, tablet or granule containing 50-500mg L-dopa methyl ester, as required. The preparation increases the dispersion degree of L-dopa methyl ester andreduces the local gastrointestinal concentration thereof, so as to reduce the side effects thereof; and at the same time, the absorption of L-dopa methyl ester is improved, so that the in vivo pharmacokinetic curve is more stable. The L-dopa methyl ester solid dispersion is a new preparation for treating Parkinson's disease.
WO2013029136A1 Tianeptine derivatives, pharmaceutical compositions, use, and method for producing same The present invention provides tianeptine derivatives, especially N-alkyl and N-alkenyl derivatives, use thereof, pharmaceutical compositions comprising same, and method for producing same. The tianeptine-derived compounds can potentially be used for treating tumours and/or psychiatric disorders.
EP2099461A2 Lna nucleoside phosphoramidates The invention provides for a compound of formula I for use in medicine: (Formula I).
WO2011010000A1 Antiviral and retroviral composition, in particular for treating aids The invention relates to compositions having antiviral properties, in particular antiretroviral properties for treating AIDS. The invention also relates to a method for producing same. The compositions of the invention are characterized in that they are developed from acetic acid and coconut extracts, a solution of mineral salts, and extracts from the Cactaceae, Liliaceae, Anacardiaceae and Euphorbiaceae families.
CN101590074A Application of carbomer gel in prevention of allergic rhinitis The invention discloses a method for preparing carbomer gel and an application thereof in allergic rhinitis. The invention provides a concrete method for preparing gel by using carbomer, flavouring peppermint oil and a neutralizing agent, such as sodium bicarbonate. The invention discovers and proves that the carbomer gel which is smeared on the mouths of nasal cavities can adsorb allergic substances, such as pollen, dust mites, and the like, and can prevent and lighten the generation of perennial and seasonal allergic rhinitis.
WO2005011710A1 Per-6-aminosubstituted-deoxy-cyclodextrins to treat alzheimer’s diseases Per-6-substituted-per-6-deoxy-cyclodextrins and compositions containing the same are disclosed. The compounds and compositions inhibit the formation and/or activity of soluble beta-amyloid-peptide derived oligomers, and can be used to treat diseases and conditions wherein such inhibition is beneficial, for example, Alzheimer's and related disease.
US20120157411 2-amino-4-arylthiazole compounds as trpai antagonists The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
CN101214326B External medicament for treating acne The present invention discloses a medicine for curing acene. The prescription of the medicine inclydes 6.5 portions of sulfur, 3.5 portions of pearl, 2.5 portions of rhizoma typhoon, 9 portions of radix saposhinikoviae, 4.5 portions of radix angelicae formosanae, 5 portions of Mongolian snakegourd kernel, 4.5 portions of Buthus martensi kirsch, 2.5 portions of periostracum cicadae, 3.5 portions ofryby sulphur, 12 portions of Yuanqing, 12.5 portions of Rhus hypoleuca, 13 portions of forrest wintergreen root and 18 portions of Glochidion eriocarpum Champ. The medicine for curing acene providedby the present invention has the characteristics of obvious curing effect, no side effect to facial skin, no allergy, no scar after cure and sameness with health skin. The efficiency is 100 percent and the curing rate is 97.8 percent. The medicine provided by the present invention with simple manufacturing process is an ideal medicine for curing acene.
CN101244048B Chalcone compounds and uses of the composition The invention discloses the application of chalcone ketones compound and the salt as shown in formula I in inhibiting cell mitosis; wherein, the application can produce the efficacy of inhibiting tumor or inhibiting over proliferation of cell. The invention also discloses the application of the compounds and the salt in treating tumor; the usage can play the role of inhibiting over proliferation of cell through inhibiting cell mitosis; in the formula (as shown in the figure), R1, R2, R3 and R4 can be independently selected from hydrogen, hydroxy, C1-C8 alkoxy, C1-C4 acyl and halogen.
EP1863762A1 Indole derivatives and methods of using the same The invention provides indole-4,7-dione derivatives useful for the treatment of diseases in a mammal, pharmaceutical compositions containing the same and methods of using the same in the treatment of cancer and neoplastic diseases including human solid tumors and other mammalian tumors.
US20080175917 Microparticles containing a H+,K+-ATP-ase inhibitor A method for the preparation of homogenous microparticles containing a H+, K+-ATP-ase inhibitor using a fluid-bed granulation technique. The microparticles that have a desired size distribution are selected. At least 80% of the microparticle based on its dry weight content is the acid labile H+, K+-ATP-ase inhibitor.
WO2009001915A1 Substituted imidazole compound and use thereof Disclosed is a novel substituted imidazole compound having excellent renin inhibitory activity, which is sufficiently practical for use as a pharmaceutical product. Specifically disclosed is a compound represented by the formula (I) below or a salt thereof. (In the formula, the symbols are as defined in the description.)
US20120058202 Means and Method for Ovarian Cancer Prognosis There is provided a method for determining whether a mammalian subject having an ovarian cancer belongs to a first or a second group, wherein the prognosis of subjects of the first group is better than the prognosis of subjects of the second group, comprising the steps of: a) evaluating an amount of RBM3 protein in at least part of a sample earlier obtained from the subject and determining a sample value corresponding to the evaluated amount; b) comparing said sample value with a predetermined refer-ence value; and if said sample value is higher than said ref-erence value, c1) concluding that the subject belongs to the first group; and if said sample value is lower than or equal to said reference value, c2) concluding that the sub-ject belongs to the second group. Related peptides, affinity ligands, uses and further methods are also provided.
CN103641767A Substituted phenylindolyl selenide, selenoxide, selenone and application as tumor cell proliferation inhibitor Belonging to the technical field of medicines, the invention relates to substituted phenylindolyl selenide, selenoxide and selenone compounds, the structural general formula of which is shown as the following, wherein each substituent group is defined in the specification. The invention also provides pharmaceutically acceptable salts and hydrates thereof formed by compounds shown as the structural formula. The pharmaceutically acceptable salts include salts formed by the derivatives and acids. Pharmacological activity test results show that, the derivatives have good antitumor activity, and can be applied as a tumor cell proliferation inhibitor in preparation of tumor drugs.
USRE39616 Aminoindan derivatives This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
EP1581543A2 Methods of producing c-aryl glucoside sglt2 inhibitors Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
CN102920872A Production method of externally-applied drug containing purslane The invention provides an externally-applied liniment for small wounds. The externally-applied liniment mainly comprises purslane, Sichuan coptis, Fructus Cnidii, dragon's blood, borneol and tea oil, and is characterized in that the externally-applied liniment is obtained through directly using ethanol as a solvent and extracting in a reverberated ultrasonic environment to obtain an extractum.
WO2012040242A1 Substituted proline inhibitors of hepatitis c virus replication The embodiments provide compounds of the general Formulae I, la, II,IIa,III, IIIa, Illb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.
US20120214873 Cysteine for physiological injection This application describes methods of making and using physiological cysteine solutions useful for reversing a neuromuscular blockade caused by a cysteine-reversible neuromuscular blockade agent, that overcomes problems of cysteine precipitation and dimerization.
US7288564 Analgesics, antiinflammatory agents, autoimmune diseases, bone disorders, central nervous system disorders Compounds of formula (I) or salts or solvates thereof or physiologically functional derivatives thereof are potent binders at the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.
CN101756984A Application of pyrro-quinoline quinine in treating and preventing atherosclerosis The invention provides an application of pyrro-quinoline quinine in treating and preventing atherosclerosis and also provides a health-care product composition or a medical composition containing pyrro-quinoline quinine. The pyrro-quinoline quinine can suppress the oxidization of low-density lipoprotein, protect endothelial cells and reduce the content of lipid in endothelium and the area of atheromatous plaques, thus the pyrro-quinoline quinine has good application prospect in preventing and/or treating the forming and the development of the atherosclerosis.
CN103382182A Phenylurea coupling quinazoline compound, and preparation method, pharmaceutical composition and pharmaceutical use thereof The invention provides a phenylurea coupling quinazoline compound or a pharmaceutically acceptable salt thereof represented by formula (I), wherein R1 represents H, represents Br, Cl or F, represents -CH3, -CH2-CH3, -CH2(CH3)2 or -CF3, represents -O-CH3, -O-CH2-CH3 or -O-CH2(CH3)2, or represents -C[triple bond]CH or -C[triple bond]N; n1 is 1, 2, 3, 4 or 5; one of R2 and R3 is a group represented by formula (II); R4 represents H, represents Br, Cl or F, represents -CH3, -CH2-CH3, -CH2(CH3)2 or -CF3, represents -O-CH3, -O-CH2-CH3 or -O-CH2(CH3)2, represents -NH2, or represents -NO2; n2 is 1, 2, 3, 4 or 5; and the other one of R2 and R3 represents H, -O-CH3, -O-CH2-CH3, -O-CH2(CH3)2, or the following groups.
EP1762568A1 Pyrazole derivatives A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, and sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group, a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.
EP2635273A2 Isoflavonoid compositions and methods for the treatment of cancer Provided herein is a pharmaceutical composition comprising an isoflavonoid derivative and a cyclodextrin. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions. In specific instances, provided herein are intravenous compositions and therapies.
CN101711841A Externally-applied liquor for treating dermatosis and preparation method thereof The invention belongs to a Chinese patent medicine which relates to externally-applied liquor for treating dermatosis and a preparation method thereof. The externally-applied liquor is prepared from Lightyellow Sophora Root, amur corktree bark, cnidium fruit, broom cypress fruit, radix sileris, honeysuckle, stemona root, pseudolarix, camphor, dittany bark, bitter peony bark, saffron crocus, ginseng, dandelion, sea buckthorn fruit, semen coicis, wrinkled gianthyssop, mulberry leaf, radix puerariae, bezoar, liaogewang, cassia nomame thorn, centipede and toad venom. The liquor has a very strong killing and preventing action to the bacteria and the fungi of staphylococcus aureus, colibacillus, candida albicans, pseudomonas pyocyanea, mould fungus and the like. The liquor has unique curative effect to the dermatosis of psoriasis, dermatitis, acne, beriberi, onychomycosis and the like. The liquor has little possibility of relapse after recovering and lower cost and can be accepted by all the common people. By clinic, feedback and follow-up survey, the total effective rate of the invention reaches more than 94%.
CN103450336A KRGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones and their preparation method, antithrombotic effect and use The invention discloses KRGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones, which are three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD peptide and are shown in the general formula I. In the general formula I, R represents Lys-Arg-Gly-Asp-Val, Lys-Arg-Gly-Asp-Phe or Lys-Arg-Gly-Asp-Ser. The invention also discloses heterocyclic nucleuses of the novel conjugates, wherein R represents OH. The invention also discloses a preparation method and in-vitro anti-platelet aggregation effects of the novel conjugates, and also discloses an antithrombotic use of the novel conjugates in a rat thrombus formation model. A result shows that the three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD peptide (wherein R represents Lys-Arg-Gly-Asp-Val, Lys-Arg-Gly-Asp-Phe or Lys-Arg-Gly-Asp-Ser) and their heterocyclic nucleuses (wherein R represents OH) have good antithrombotic activity and clear application prospects in antithrombotic agent preparation.
EP2060264A1 Agent for treating eye diseases The invention relates to chemical and pharmaceutical industry, in particular to developing ophthalmological agents having a wide spectrum of action based on vegetable components, vitamins, and trace elements. The agent for treating eye diseases comprises lyophilized blueberries, dihydroquercetin, beta-carotene, selexen, lutein, vitamins B1, B2, B6, and B12, and zinc. The agent having a wide spectrum of action exhibits a reparative, restorative (tonic) and regenerative effect, it does not have any irritating, allergenic, inflammatory or other undesirable effect, and it avoids mechanical contact with the eye surface.
CN101129364A Use of protoberberine alkaloid in preparing against bacterial resistance medicament The invention discloses an application of protoberberine alkaloid to prepare anti-drug tolerant bacterial drug, in particular to an application of compound coptisine, dehydrokaweidin and dihydroapokaweidin in the anti-drug tolerant bacterial drug, which is characterized by the following: extracting protoberberine from Corydalis saxicola Bunt. of Corydalis of Papaveraceae; displaying obvious inhibition for MRSA in the clinic through pharmacological test; using the compound protoberberine alkaloid as active component to make the drug to treat anti-drug tolerant bacterial drug.
US20080261976 Novel piperidinecarboxamide derivatives, method for preparing same and pharmaceutical compositions containing same The invention relates to compounds of formula (I): as well as their salts with inorganic or organic acids, their solvates and/or their hydrates, which exhibit a very high affinity both for the human NK2 receptors for neurokinin A and for the human NK3 receptors for neurokinin B and are antagonists of the said receptors. The invention also relates to their method of preparation, the pharmaceutical compositions containing them and their use for the preparation of medicaments.
WO2007088438A2 Benzisoxazole oxazolidinones as antibacterial agents The present invention provides a compound of Formula (I) Or a pharmaceutically acceptable salt thereof wherein: W is CH2NHC(=Z)R1, C(=Z)NHR2, or CH2het; X is H, C1-6alkyl, or C2-6alkenyl; Y is H, or F; Z is O, or S; R1 is C1-6alkyl, NHC1-6alkyl, C3-7cycloalkyl, C2-6alkenyl, or OC1-4alkyl; R2 is H, C1-4alkyl, or -OC1-4alkyl; and het is a five-(5) or six-(6) membered heterocyclic ring having 1-4 heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen within the ring, wherein each carbon atom in het is optionally substituted with C1-4alkyl, C2-4alkenyl, C2-4alkynyl, halo, OR3, CN, NO2, NHR3R3, oxo, CF3, OCF3, C(=O)C1-4alkyl, OC(=O)C1-4alkyl, or C(=O)OR3; wherein R3 is H, or C1-4alkyl.
CN101091717A Medicine to lower the temperature in use for pigs and preparation method The present invention relates to an animal medicine and its preparation method, in the concrete, it relates to a swine antipyretic medicine. It is an injection preparation for effectively curing innominate high fever of swine. Said medicine is made up by using 40-60 ml of mancozeb, 2-8 ml of doxycycline hydrochloride powder and 38-50 ml of astragalus polysaccharide injection. Besides, said invention also provides the concrete steps of its preparation method.
EP1326617B9 Use of 11beta-(4-acetylphenyl)-17beta-hydroxy-17alpha-(1,1,2,2-pentafluoroethyl)estra-4,9-dien-3-one for the preparation of a medicament for the treatment fo breast, ovarian, endometrial cancer, myeloma and meningioma The present invention relates to methods and uses for inducing apoptosis in a cell, in particular a breast cancer cell, by the administration of antiprogestins, in particular the antiprogestin 11 beta -(4-acetylphenyl)-17 beta -hydroxy-17 alpha -(1,1,2,2,2-pentaf luoroeth yl)-estra-4,9-dien-3-one or a pharmaceutically acceptab le derivative or analogue thereof. The invention further relates to a treatment of cancer wherein an indicator of high risk is an increased amount of tumor cells in the S-phase of the cell cycle, said treatment comprising an antiprogestin, in particular the antiprogestin 11 beta -(4-acetylphenyl)-17 beta -hydroxy-17 alpha -(1, 1,2, 2,2- pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof.
CN1795860A Oral taking chewy composition for covering unflavored taste and preparation method A chewing composition for masking the bad taste features that it contains the pharmacologically acceptable salts of organic acid or inorganic acid. Its preparing process is also disclosed.
US20110230453 Use of Female Mammal's Urine for Determination of Fetal Gender Related Characteristics The present invention provides a method for determining the gender of a fetus by assaying the sex hormones, evaluating the overall reducing/oxidizing (redox) activity, and/or evaluating the radical scavenging capacity of the maternal urine or other body fluid. The method can be used to determine fetal gender at any time point during the entire pregnancy. The body fluid may be processed before assaying. Processing may involve aging the body fluid, or purification of various fractions. The methods of the present invention also provide for a means for pre-conception offspring gender planning by assaying the sex hormones, evaluating the overall reducing/oxidizing (redox) activity, and/or evaluating the radical scavenging capacity of the urine or other body fluid from a non-pregnant female. The sex hormone profiles, the overall redox activity, and/or the radical scavenging capacity of a urine sample correlates with the gender specific compatibility of the ovum being released during a particular menstrual cycle. Therefore, assaying aforementioned parameters from a non-pregnant female's urine will help a couple or an animal breeder have an offspring of a desired gender. The present invention also provides a method of conceiving a baby of a desired gender in a female by applying to the female a pharmaceutical formulation with a specific sex hormone composition.
CN102648936A Medicinal composition for treating wound surface and preparation method and application thereof The invention relates to a medicinal composition for treating a wound surface and a preparation method and applications thereof. The medicinal composition is applied to preparation of medicaments for treating burn, scalds, wound surfaces after trauma, wound surfaces after war injury, diabetes mellitus wound surfaces, wound surfaces caused by chemotherapy and radiotherapy, wound surfaces caused by transplanting, wound surfaces caused by vascular diseases, pressure sores (bedsores), cold injury, a plurality of other unhealed/difficultly-healed wound surfaces, insect bites and the like.
WO2008064296A1 Method of treating neurological disorders with carbonic anhydrase inhibitors Described herein are methods for treating a subject, such as an animal or human, having a neurological disorder or at risk for developing a neurological disorder (e.g., a patient that has a genetic defect associated with a neurological disorder, but does not appear to suffer from any symptoms commonly associated with the neurological disorder) by administering to the subject having the neurological disorder an effective amount of a carbonic anhydrase inhibitor.
WO2010064597A1 Piperidine derivative A compound represented by formula (I) or a salt thereof. In formula (I), the symbols are as defined in the description.
WO2005005439A1 Benzothiazino indoles This invention particularly relates to novel benzothiazinoindole derivatives represented by the general formula (I), given below: wherein R1, R2, R3, R4, R5, R6,, R7, R8, R9, R10, R11, R12, R13 and R14, may be same or different and each independently represent hydrogen, halogen, oxo, thio, perhaloalkyl, hydroxy, amino, nitro, cyano, formyl, amidino, guanidino, substituted or unsubstituted groups selected from linear or branched (Cl-C,12)alkyl, (C2-C12)alkenyl, C2-C12)alkynyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkenyl, bicycloalkyl, bicycloalkenyl, C1-C12)alkoxy, cyclo(C3-C7)alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, heterocyclylalkyloxy, acyl, acyloxy, acylamino, monoalkylamino, dialkylamino, arylamino, diarylamino, aralkylamino, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, heterocyclylalkoxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonyamino, aryloxycarbonylamino, dialkylaminocarbonylamino, alkylamidino, alkylguanidino, dialkylguanidino, hydrazino, hydroxylamino, carboxylic acid and its derivatives, sulfonic acids and its derivatives, phosphoric acid and its derivatives; or two adjacent groups may form 'cyclic structures', for example, R1 and R2, R2 and R3, R5 and R6, R6, and R7, R7 and R8 together with the adjacent carbon atoms to which they are attached may form a 5, 6, or 7 membered ring, which may further optionally contain one or more double bonds and/or one or more heteroatoms such as the group 'Oxygen', 'Nitrogen' 'Sulfur' or 'Selenium' and combinations of double bond and heteroatoms; or R9 and R10 or R11 and R12 or R13 and R14 together represent double bond attached to 'Oxygen' or 'Sulfur'; or two adjacent groups may form 'cyclic structures' for example, R11 and R12, Ril and R13, R11 and R14, R13 and R14 together with the carbon atom/s to which they are attached may form a 3, 4, 5, or 6 membered ring, which may further optionally 10 contain one or more double bonds, and/or one or more heteroatoms such as the group 'Oxygen', 'Nitrogen', 'Sulfur' or 'Selenium' and also includes combination of one or more double bonds with 'heteroatoms', as above defined, R15 and R16 may be same or different and each independently represents hydrogen, substituted or unsubstituted groups selected from linear or branched (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkenyl, bicycloalkyl, bicycloalkenyl, aryl, aralkyl, heteroaryl, heterocyclylalkyl; optionally R15 and R16 along with the nitrogen atom may form a 3, 4, 5, 6 or 7 membered heterocyclic ring, which may further optionally contain one or more double bonds, and may include additional one or more heteroatoms such as the group 'Oxygen', 'Nitrogen', 'Sulfur' or 'Selenium' and also includes combination of one or more double bonds with 'heteroatoms', as above defined; 'n' ranges from 0 to 4, wherein the carbon chains which 'n' represents may be either linear or branched.
WO2014121634A1 Novel bacterial colony sensing regulator and medical use A compound in formula I, and a preparation method and use thereof. The compound has a function of sensing and regulating a bacterial colony, and can be used for prevention and/or treatment of related diseases caused by bacterial infection.
CN102977413A New method for preparing micelles by compounding polymers A new method for preparing micelles by compounding polymers, belongs to the technical field of biomedical materials. Alginic acid and poly (2-(N, N-dimethyl)amino ethyl methacrylate (PDMAEMA) are compounded in an aqueous solution, and nanomicelles are formed via electrostatic interaction between the carboxyl group of the alginic acid and amino group of PDMAEMA. By using different molar ratios of the carboxyl group and the amino group for compounding, experimental results show that the best effect is obtained when the ratio of the two groups is 1:1, and the obtained micelles has structured morphology and narrow particle size distribution. The advantages of the present invention are: the method for preparing micelles is simple and no use of organic solvents; and the micelles obtained are good in biocompatibility and biodegradable. The micelles can be used as a drug carrier which has a good release effect under simulated human body physiological conditions.
WO2014050717A1 Skin condition amelioration agent The present invention effectively ameliorates deterioration in skin condition in terms of sagging, texture, firmness, or the nasolabial folds arising with age. To said end, the present invention uses 1) collagen peptides, 2) proteoglycans, and at least one selected from 3) a bloodflow promoting substance, 4) an antioxidant substance, and 5) an estrogen-like substance.
CA2842550A1 Intravaginal devices for drug delivery Intravaginal drug delivery devices, including intravaginal rings, are provided herein. The devices include a reservoir of at least one vaginally administrable drug wherein the reservoir is surrounded at least in part by a hydrophilic elastomer. The devices are capable of exhibiting a substantially zero order release profile of drug over extended periods of time. Also disclosed are methods for making the devices and methods of using the devices to prevent or treat a biological condition.
CN103536551A Fluorouracil composition freeze-dried powder for injection The invention provides a fluorouracil composition freeze-dried powder for injection, and belongs to the field of medicine and medicine preparation technology. The fluorouracil composition freeze-dried powder comprises following raw material ingredients, by weight, 9.26 to 11.16 parts of fluorouracil, 4.63 to 5.58 parts of chitosan nanoparticle, and 84.35 to 88.56 parts of injection water. Advantages of the fluorouracil composition freeze-dried powder are that: the fluorouracil composition is made into freeze-dried powder, so that solubility is high, and stability of the fluorouracil composition freeze-dried powder is higher than that of common fluorouracil water-based injection; utilization safety is ensured, and validity term is prolonged because of the excellent solubility and stability.
CN102973590A Application of alginic acid in preparing medicament for treating hepatic fibrosis The invention discloses novel application of alginic acid in preparing a medicament for treating hepatic fibrosis. The medicament can be used for inhibiting inflammatory reaction in hepatic fibrosis attaching process, so that attack or symptom worsening of hepatic fibrosis can be inhibited. Alginic acid has good curative effect in a carbon tetrachloride induced animal model; and the medicaments used in the application can be easily acquired, low in price and stable in properties, are convenient to store and transport, and have wide application prospect.
CN103463029A Application of Lycojaponicumin B in human fungus resisting medicine The invention relates to an application of Lycojaponicumin B in preparation of a human fungus resisting medicine, belonging to the field of medicines. The Lycojaponicumin B has strong effects of inhibiting trichophyton rubrum, Microsporum lanosum or Trichophyton tonsurans, therefore, the Lycojaponicumin B can be used as a compound with a human fungus resisting function, and is expected to be applied in the preparation of the related medicines. The application of the Lycojaponicumin B in preparation of the human fungus resisting medicine, disclosed by the invention, is disclosed for the first time. The skeleton type of the Lycojaponicumin B belongs to a brand-new skeleton type, and the human fungus inhibiting activity of the Lycojaponicumin B is unexpectedly strong, so that no possibility for providing any inspiration by other compounds exists. The Lycojaponicumin B has outstanding substantial characteristics, meanwhile, has a significant progress in prevention and treatment of human fungal infection.
WO2013111823A1 Method for producing sphingoid base-containing extract [Problem] To provide a method for producing a sphingoid base-containing extract, and a functional food or pharmaceutical composition containing the resulting extract. [Solution] This method for producing a sphingoid base-containing extract comprises: (1) a step for extracting lipids, including sphingolipids, from a natural product; (2) a step for chromatographically fractionating from the extract obtained in step (1) to obtain glycosphingolipids; and (3) a step for acid-hydrolyzing the glycosphingolipids and subsequently extracting and removing fatty acid methyl ester and free fatty acid from the hydrolysate. The resulting extract has a high intestinal hormone secretagogue function per calorie or per molecule (per number of moles), and is less readily absorbed from the intestinal tract, and is therefore useful as a functional food or pharmaceutical active ingredient that can be made available for preventing or treating obesity, diabetes, or enteropathy.
CN103157117A Medicine for regulating and controlling TRAIL (Tnf (Tumor necrosis factor) Related Apoptosis Inducing Ligand) tolerance of tumour The invention relates to a medicine for regulating and controlling the TRAIL (Tnf (Tumor necrosis factor) Related Apoptosis Inducing Ligand) tolerance of tumour. The medicine comprises microRNA (Ribose Nucleic Acid) shown in sequence (SEQ) IDNO.1-4 and variants thereof; the microRNA shown in the SEQ IDNO.1-2 is combined with a death receptor (DR) 5 gene 3'-UTR to inhibit the expression of the DR5 gene and improve the TRAIL tolerance of tumour; and the microRNA shown in the SEQ IDNO.3-4 is not combined with the DR5 gene 3'-UTR to improve the expression of the DR5 gene and reduce the TRAIL tolerance of tumour. The purpose of regulating and controlling the TRAIL tolerance of tumour cells is achieved through regulating and controlling the DR5 gene expression by using the microRNA.
US20120289574 Hydrate crystals New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals.
US20110319807 Rejuvenation or preservation of germ cells Certain embodiments disclosed herein include, but are not limited to, at least one of compositions, methods, devices, systems, kits, or products regarding rejuvenation or preservation of germ cells or gametes. Certain embodiments disclosed herein include, but are not limited to, methods of modifying germ cells or gametes, or methods of administering modified germ cells or gametes to at least one biological tissue.
US20080058345 Combination Therapy with Mecamylamine for the Treatment of Mood Disorders A combination therapy for treating mood disorders, including depressive disorders such as major depression, panic disorder, obsessive compulsive disorder, social anxiety disorder, seasonal affective disorder, and premenstrual dysphoria is provided herein. The combination therapy comprises administering an effettive amount of mecamylamine together with at least one agent for treatment of a mood disorder to a patient in need of treatment of the mood disorder. Pharmaceutical formulations, including packaged pharmaceutical formulations, comprising mecamylamine and an additional agent, such as an SSRI, are also provided herein.
EP1914229B1 Novel cercosporamide derivative The invention relates to a novel cercosporamide derivative which has a good hypoglycemic effect and is useful for a therapeutic drug and/or preventive drug for diabetes, a pharmacologically acceptable salt thereof or an ester thereof. [MEANS FOR SOLVING PROBLEMS] The cercosporamide derivative having the general formula (I): (wherein X represents an oxygen atom or the like, R1 represents a hydrogen atom or a C1-C6 alkyl group, R2 represents a hydrogen atom, a C1-C6 alkyl group or a C1-C6 halogenated alkyl group, R3 represents a hydrogen atom or a C1-C6 alkyl group, R4 represents a C6-C10 aryl group which may be substituted with 1 to 5 groups independently selected from the substituent group (a) or the like, n represents 1, 2 or 3, and the substituent group (a) represents a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 alkoxy group, a C1-C6 halogenated alkoxy group, a C2-C6 alkenyloxy group, a C2-C6 alkynyloxy group and the like), a pharmacologically acceptable salt thereof or an ester thereof.
US20100173865 Anti-Cancer Agent-Hyaluronic Acid Conjugate Compositions and Methods Methods of making conjugates comprising an anti-cancer agent and hyaluronic acid, together with mixtures of reaction products comprising such conjugates and methods of using such conjugates in therapeutic and research applications are disclosed.
EP1845097A1 Oxadiazole derivatives as COMT inhibitors This invention relates to novel substituted [1,2,4]-oxadiazoles, their use in the treatment of some central and peripheral nervous system disorders, methods for their preparation and pharmaceutical compositions containing them.
US7115658 Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus. Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus
CN1527704B Compositions and method of administering tubulin binding agents for the treatment of ocular diseases The present invention is directed to the administration of vascular targeting agents, particularly a tubulin binding agent, for the treatment of ocular neovascularization, ocular tumors, and conditions such as diabetic retinopathy, retinopathy of prematurity, retinoblastoma and macular degeneration.
CA2383212C Controlled release oral dosage suitable for oral administration The present invention is directed to a pharmaceutical composition, preferably in the form of a tablet comprising a therapeutically effective amount of a medicament in a carrier comprising a water insoluble polymer and a water-insoluble inorganic salt.
WO2005009468A1 Remedy for cartilage-related diseases A remedy for cartilage-related diseases containing as the active ingredient a substance having an agonistic activity to EP2 and/or EP3. A substance having an agonistic activity to EP2 and/or EP3 has effects of promoting chondrogenesis, promoting chondrocyte growth, promoting chondrocyte differentiation, inhibiting cartilage calcification and inhibiting cartilage degradation, or effects of promoting integrin mRNA expression, promoting fibronectin mRNA expression, promoting cyclin D1 mRNA expression and inhibiting osteopontin mRNA expression, and, therefore, is useful as a remedy for cartilage-related diseases.
CN101130065A Soft capsule of pearl calcium and method of preparing the same The invention discloses a soft capsule of pearl calcium and scientific making method that makes the calcium in the pearl to be a secure supplementary calcium agent for human body's because of the calcium in the pearl not easy to be absorbed, wherein raw material is ultramicro pearl powder, casein phosphopetide calcium chelating, corn oil, casein phosphopetide, fish liver oil and vitamin D. The invention has supplementary calcium effect through the experiment of feeding the rat with low calcium feeding-stuff and the invention for 3months respectively. Compared with the low calcium team, the product has much distinctive differences for the femoral bone factor and the femoral bone calcium content, and has the much distinctive difference in comparison with the calcium carbonate team. Utilizing the two indexes of the bone calcium content and the femoral bone factor to compare with the same calcium ion dosage of the calcium carbonate team, the product is superior to the calcium carbonate team in increasing the bone calcium content and weight.
US20110124565 Modified Coagulation Factor VIII With Enhanced Stability and Its Derivatives The present invention relates to modified nucleic acid sequences coding for coagulation factors, in particular human Factor VIII and their derivatives with improved stability, recombinant expression vectors containing such nucleic acid sequences, host cells transformed with such recombinant expression vectors, recombinant polypeptides and derivatives which do have biological activities of the unmodified wild type protein but having improved stability and processes for the manufacture of such recombinant proteins and their derivatives. The invention also covers a transfer vector for use in human gene therapy, which comprises modified DNA sequences.
US20100273868 R-Zileuton for Use in Conditions Associated with Increased 5-Lipoxygenase and/or Leukotriene Activity (EG Asthma) The invention pertains to a method of treating a condition mediated by or characterized by increased 5-lipoxygenase activity like for instance asthma in a patient suffering therefrom comprising administering to said patient a composition comprising (R)-zileuton and a pharmaceutically acceptable excipient, wherein said composition is substantially free of (S)-zileuton.
US7250430 Administering N-benzoyl- derivatives, e.g., N-[2,4-dichlorobenzoyl]-5-bromothiophene-2-sulfonamide sodium salt, to treat metastatic soft tissue sarcoma, non-small cell lung cancer, melanoma, ovarian cancer, breast cancer, leukemia, lymphoma, renal cancer, prostate cancer, and multiple myeloma The present invention provides antineoplastic compounds of the formula: and antineoplastic methods.
US7132553 Inhibitor is a (2-amino-(optionally -1-oxo)-3-thiopropyl)--5,6,7,8-tetrahydroimidazo[1,2a]pyrazine derivative or its disulfide dimer, e.g., (2-amino-1-oxo-3-thiopropyl)-8-(cyclohexylmethyl)-2-phenyl-5,6,7,8-tetrahydroimidazo[1,2a]pyrazine A composition comprising at least one G protein inhibitor of the formula wherein the substituents are defined as in the specification and the salts thereof and at least one other antihypertensive agent for the treatment of arterial hypertension.
WO2012035406A1 Tryptamine derivatives, their preparation and their use in gastropathy The present invention concerns the synthesis and evaluation of gastroprotective effect of different tryptamine derivatives. Tryptamine derivatives have been synthesized by formation of amide or ester with some known anti oxidant molecules. These derivatives show excellent antioxidant property in vitro. Among all the derivatives the compound SEGA (3 a), that was prepared by the combination of serotonin with gallic acid shows the greater antioxidant property than the other synthesized compounds both in vivo and in vitro. SEGA(3a) shows the gastroprotective effect against NSAIDs (indomethacin or diclofenac)-induced gastropathy in dose dependent manner and also accelerates the healing from injury. It prevents the NSAIDs-induced mitochondrial oxidative stress in vivo. This derivative prevents NSAID-induced mitochondrial oxidative stress-mediated apoptosis in vivo by preventing the activation of caspase 9 and caspase-3 and restores NSAIDs-mediated collapse of mitochondroial transmembrane potential and dehydrogenase activity. SEGA (3 a) plays an important role as an iron chelator as well as intra mitochondrial ROS scavenger. Thus, SEGA (3 a) is a potent antioxidant antiapototic molecule, which efficiently prevents NSAID-induced gastropathy and stress or alcohol -mediated gastric damage.
CA2146707C Substituted n-heteroaroylguanidines as inhibitors of na+/h+ exchange The invention relates to heteroaroylguanidines of the Formula I (see formula I) in which the substituents HA and R(1) to R(5) have the meanings given in claim 1. These compounds exhibit very good antiarrhythmic properties, as are important for treating diseases which occur, for example, in association with symptoms of oxygen deficiency. As a consequence of their pharmacological properties, the compounds are outstandingly suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias. On account of their protective effects against pathological hypoxic, and ischemic situations, the compounds of the formula I according to the invention can, as a consequence of inhibiting the cellular Na+/H+ exchange mechanism, be used as pharmaceuticals for treating all acute or chronic damage elicited by ischemia, or diseases induced primarily or secondarily thereby. This is the case with regard to their use as pharmaceuticals for surgical interventions, for example in organ transplantations, where the compounds can be used both for protecting the organs in the donor prior to and during removal, for protecting organs which have been removed, for example when they are being treated with or stored in physiological bathing fluids, and when transferring the organs into the recipient. The compounds are likewise valuable protective pharmaceuticals to be used when carrying out angioplastic surgical interventions, for example on the heart or on peripheral vessels. In conformity with their ability to protect against ischemically induced damage, the compounds are also suitable for use as pharmaceuticals for the treatment of ischemias of the nervous system, in particular of the CNS, in connection with which they are suitable, for example, for the treatment of stroke or cerebral edema. Over and above this, the compounds of the formula I according to the invention are also suitable for use in the treatment of forms of shock, such as, for example, allergic, cardiogenic, hypovolemic and bacterial shock.
WO2008006276A1 THE SMALL MOLECULE INHIBITOR WHICH CAN INHIBIT THE AβPOLYPEPTIDE FIBROSIS OF ALZHEIMER'S DISEASE, THEIR PREPAREATION METHODS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF A type of novel compounds having the symmetric structure of formula I, which can inhibit the congregation and fibrosis of β-amyloid protein, their pharmaceutically accepted salts, and preparation methods thereof. The pharmaceutical compositions containing these compounds or their pharmaceutically accepted salts, and the uses of these compounds or their pharmaceutically accepted salts or their pharmaceutical compositions for the manufacture of a medicament for the prevention or treatment of an Alzheimer's disease. The compounds or their pharmaceutically accepted salts discloses in present invention can inhibit the congregation and fibrosis of β-amyloid protein by combining with Aβ polypeptide. So they can be used to prevent or treat Alzheimer's diseases.
CN101095946A Anti-drug liquor for giving up drug-taking and method for preparing the same The invention discloses a kind of drug rehabilitation liquor, which comprises 83% SOD solution and 17% anthocyanins solution (ratio by volumetric). Said SOD solution is extracted from compound that comprises white camellia 90-110 and ledum palustre terpenes 8.5-10.5 (ratio by weight). Said anthocyanins solution contains 25-39% of natural wild slurry anthocyanins. The product can reduce addiction action in brain for drug user and eliminate dependence on drug, which is characterized by good effect, no anesthesia component, no dependence effect, non-toxic, convenient intake and fast absorption, and effective protection for liver, heart, brain and kidney. The invention also provides a method for preparing said drug rehabilitation liquor.
US7816376 Use as excitatory amino acid antagonists for combating neurodegenerative and cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, or psychoses; for example, 3-[4-(3,4-methylenedioxybenzyl)piperidino]-N-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propionamide The invention relates to compounds of the formula (I) and pharmaceutically usable derivatives, salts, solvates and stereoisomers and mixtures thereof, in which X, Y, Z, R1, R3, R4, R8, p, k, E, G, Z and Q are as defined in claim 1, which are employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, cerebral ischaemia, infarction or psychoses.
EP2303249A2 Anthraquinones and analogs from rhuem palmatum for treatment of estrogen receptor beta-mediated conditions Compositions derived from Rheum palmatum are provided. Also provided are methods of using said extracts to induce apoptosis in specific cells, especially in a human. Provided as well are uses of the extracts of Rheum palmatum for the preparation of a medicament for the selective induction of apoptosis.
CN101768182A Acetylpyridine-5-chloric salicylacylhydrazone dibutyltin dichloride coordination compound and preparation method and application thereof The invention discloses acetylpyridine-5-chloric salicylacylhydrazone dibutyltin dichloride coordination compound, the structural formula of which is as follows. The preparation method comprises the following steps: adding 1.5-2.0mmol of acetylpyridine-5-chloric salicylacylhydrazone, 3.0-4.0mmol of sodium methoxide and 50ml of absolute methanol into a round bottom flask, stirring for 0.5h, then adding 2.0-3.0mmol of dibutyltin dichloride, and stirring for 6-8h at the normal temperature; filtering, evaporating the filter liquor through rotation, obtaining yellow solids, performing recrystallization through dichloromethane-absolute ethyl alcohol with the volumetric ratio of dichloromethane to absolute ethyl alcohol of 1:1, and obtaining yellow crystal which is the organic tin acylhydrazone coordination compound. The coordination compound has high anticancer activity, can be used to prepare medicines for treating liver cancer and cervical carcinoma of human as the raw material, and has the advantages of high anticancer activity, good fat solubility, low cost and simple preparation method than the platinum anticancer drugs commonly used at present.
WO2013072882A1 2 -amino- 1, 8 -naphthyridine-3 -carboxamide derivatives as antimicrobial agents The present invention concerns novel 2-amino-1,8-naphthyridine-3-carboxamide derivatives of formula I, a pharmaceutical antibacterial composition containing them and the use of these compounds in the manufacture of a medicament for the treatment of infections (e.g. bacterial infections). These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.
WO2009119652A1 USE OF BENZOPHENONE DERIVATIVE OR SALT THEREOF AND TNF α INHIBITOR IN COMBINATION AND PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVE OR SALT THEREOF AND THE INHIBITOR Disclosed are use of a benzophenone derivative represented by general formula (I) or a salt thereof and one or more TNFα inhibitors in combination, and a pharmaceutical composition containing the benzophenone derivative or a salt thereof and one or more TNFα inhibitors. The use and the composition are useful for treatment or prevention of autoimmune diseases and the like. (In the formula, R1 represents an optionally substituted heterocyclic group, a substituted phenyl group or the like; Z represents an alkylene group or the like; R2 represents a carboxyl group, which may be protected by an alkyl group, or the like; R3 represents an optionally protected hydroxyl group or the like; R4 represents an optionally substituted cycloalkyloxy group or the like; and R5 represents a hydrogen atom or the like.)
CN103356590A Application of Sarcaboside A in thrombocyte-increasing medicines The invention relates to new application of a compound Sarcaboside A in the field of pharmacy, particularly application of Sarcaboside A in preparing thrombocyte-increasing medicines. The application of Sarcaboside A in preparing medicines for treating low thrombocyte is disclosed for the first time. Since the framework type is brand-new and has unexpectedly high activity for inhibiting low thrombocyte, the Sarcaboside A does not has the possibility of any inspiration given by other compounds, has outstanding substantive characteristics, and obviously has significant progress in preventing and treating low thrombocyte.
EP2766495A1 Method of diagnosis, prognostic or treatment of neurodegenerative diseases The present invention relates to a method of diagnosis, prognostic or treatment of neurodegenerative diseases, in particular Alzheimer's disease.
CN102872036A Application of Gypensapogenin A in medicament for increasing level of red blood cells The invention relates to a new application of a compound Gypensapogenin A in the pharmaceutical field. The invention relates to a new application of Gypensapogenin A in a medicament for increasing the level of red blood cells. The application of the Gypensapogenin A provided by the invention in the preparation of a medicament for treating the deficiency of the red blood cells is disclosed for the first time; and a skeleton type is a bran-new skeleton type, and the strong inhibition activity of the Gypensapogenin A on the deficiency of the red blood cells is unexpected, thus the possibility that other compounds provide any implication does not exit, the application has the outstanding substantive feature, and simultaneously, the application of the Gypensapogenin A in the prevention and treatment of the deficiency of the red blood cells is obviously improved.
US20090281116 Pyrrole derivatives, preparation thereof and therapeutic use thereof The invention relates to compounds having the formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R9 and A-R9 are as defined herein. Also disclosed are the preparative methods for the compounds of formula (I) and their use in therapy.
US20050054587 Novel therapeutic indication of azithromycin for treatment of non-infective inflamatory diseases The invention relates to the use of 9-deoxo-9-dihydro-9a-methyl-9a-homoerythromycin. A (generic name: azithromycin) for the therapy of neutrophil-dominated non-infective inflammatory diseases, pharmaceutical compositions containing azithromycin for enteral or parenteral administration and methods for the production of these pharmaceutical compositions.
US20050164979 Pharmaceutical composition for ophthalmological and rhinological application The invention concerns a pharmaceutical composition which contains at least panthenol and/or pantothenic acid and hyaluronic acid and/or hyaluronate and optionally additionally pharmaceutical auxiliary agents. The invention further concerns the use of the pharmaceutical composition for the treatment of ophthalmological and/or rhinological malfunctions.
WO2006008470A3 Treatment of tumours The present invention provides the use of a metal ion chelating agent for the manufacture of a medicament for the treatment or prophylaxis of a bacteria-mediated cancerous tumour, wherein said metal ion chelating agent provides a metal ion chelating capacity for at least one metal ion on which said tumorigenic bacteria is dependent for viability. The invention also provides methods for the treatment or prophylaxis of tumours.
WO2010045656A3 Novel sglt2 inhibitor dosage forms A pharmaceutical composition comprising a sodium-dependent glucose transporter (SGLT2) inhibitor and a biguanide, wherein at least one of the active agents is in slow release form, is provided. A method for treating diabetes in a patient in need thereof including administering an anti-diabetic combination comprising a sodium- dependent glucose transporter (SGLT2) inhibitor and a biguanide, wherein at least one of the active agents is in slow release form, is also provided.
CN103641828A Triazolonaphthyridine-one derivative compound and preparation method and application thereof The invention relates to a triazolonaphthyridine-one derivative compound and a preparation method and application thereof, belonging to the technical field of drug synthesis. In order to solve the problems that the prior art is only limited to the change of different substituent groups on a naphthyridine ring and the study on the ring combination of naphthyridine rings and the activity of corresponding derivative compounds is still not reported, the invention provides a triazolonaphthyridine-one derivative compound and a preparation method and application thereof. The method comprises the following steps: performing a substitution reaction between the compound 2,3-diamino-4-phenyl-2,7-naphthyridine-1-(2H)-one of formula II and a compound aldehyde or acid anhydride of formula III at 100-200 DEG C to obtain the triazolonaphthyridine-one derivative compound. The compound provided by the invention has anti-tumor activity; the synthesis method is finished in one step, and the process step is short, thereby being favorable for industrial production.
US7820669 2-(piperidin-4-yl)-4,5-dihydro-2H-pyridazin-3-one derivatives as PDE4 inhibitors The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.
WO2007010013A3 Combination comprising a pyrimidylaminobenzamides and a flt-3 inhibitor for treating proliferative diseases The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound; and b) a Flt-3inhibitor, and a method for treating or preventing a proliferative disease using such a combination.
CN101328178B Penem derivates containing thiophen substituted sulfhydryl pyrrolidine The invention belongs to the medicine technical field, in particular relating to a penem derivate containing thiophene-substituted sulfhydryl pyrrolidine as shown in a general formula (1), a salt thereof acceptable in pharmacology, an easily hydrolyzed ester thereof, an isomer thereof, a hydrate thereof and a hydrate of the ester or the salt thereof, wherein R<1>, R<2>, R<3> and R<4> are defined in a specification. The invention also relates to a preparation method of the compounds, a medicine combination containing the compounds and an application of the compounds in preparing medicines usedto treat and/or prevent infectious diseases.
US20120064156 Pharmaceutical Compositions for the Coordinated Delivery of NSAIDs The present invention is directed to drug dosage forms that release an agent that raises the pH of a patient's gastrointestinal tract, followed by a non-steroidal anti-inflammatory drug. The dosage form is designed so that the NSAID is not released until the intragastric pH has been raised to a safe level. The invention also encompasses methods of treating patients by administering this coordinated release, gastroprotective, antiarthritic/analgesic combination unit dosage form to achieve pain and symptom relief with a reduced risk of developing gastrointestinal damage such as ulcers, erosions and hemorrhages.
CN102786469A O-pyridylhydrazide derivatives, and preparation method, medicinal composition and uses thereof The invention relates to 1-(4-chloro-3-trifluoromethylphenyl)-3-(4-(2-(2-isopropenylhydrazine carbonyl)pyridine-4-oxo)phenyl)carbamide with the structure represented by formula I and 1-(4-chloro-3-trifluoromethylphenyl)-3-(4-(2-(2-isopropylhydrazine carbonyl)pyridine-4-oxo)phenyl)carbamide with the structure represented by formula II, medicinal salts thereof, preparation methods thereof, a composition containing one or more of above compounds, and uses of the compounds in the treatment of protein kinase associated diseases, such as immune disorder and tumor diseases.
US7172769 Methylsulfonylphenyl or phenylsulfonamide derivatives having ring selected from cyclopentenone, furanone, methylpyrazole, isoxazole and pyridine; celecoxib and rofecoxib; administered for pain; oral drug delivery Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory drug of low water solubility in a therapeutically effective amount, wherein the drug is present in the form of solid particle, about 25% to 100% by weight of which are smaller than 1 μm. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders and have particular advantages where rapid onset of therapeutic effect is desired.
US20110196036 Use of betaine The present invention relates to use of betaine for protecting skin from biological irritation. The invention also relates to the use of betaine as a protecting agent in a cosmetic and/or toiletry preparation. The invention further relates to a method of protecting skin from biological irritation.
CA2651684A1 Peptide compounds for treating refractory status epilepticus The present invention is directed to the use of a class of peptide compounds for prevention, alleviation or/and treatment of refractory status epilepticus.
CN101518580A Pharmaceutical composition for clearing heat and releasing toxin as well as preparation method and application thereof The invention belongs to the field of medicament, and in particular relates to a pharmaceutical composition for clearing heat and releasing toxin as well as a preparation method and application thereof. The first technical problem to be solved is to provide the pharmaceutical composition for clearing heat and releasing toxin, and the pharmaceutical composition comprises the following components by weight portion: 8 to 12 portions of chrysanthemum, 6 to 10 portions of honeysuckle flower, 8 to 12 portions of Grosvener Siraitia, 2 to 6 portions of unripe chebule, and 2 to 6 portions of cape jasmine fruit; and the five medicaments synergistically have efficacies in dispelling wind, clearing heat, discharging fire and releasing toxin. In order to achieve the aims of clearing fire and not injuring Yin and improve the clearing effect of the medicaments, the pharmaceutical composition is also added with adenophora, greenish Lily bulb, Indian buead, coix, cassia seed and hawthorn fruit, and additionally aided with common floweringquince fruit, Chinese angelica, radix astragali seu hedysari and menthol for clearing heat and discharging fire, strengthening healthy energy and beautifying, invigorating blood circulation and removing blood stasis. The pharmaceutical composition can be used for improving symptoms such as stomatoglossitis, abscess of throat, halitosis, gingival bleeding, acne, irritation and insomnia, constipated, colored patches, cough, expectoration, obesity or hyperlipemia, and has no side effects such as diarrhea, stomachache and anorexia after being taken for a long time.
US20120328704 Powder compositions for inhalation The present invention relates to newly identified genes that encode proteins that are involved in the synthesis of L-ascorbic acid (hereinafter also referred to as Vitamin C). The invention also features polynucleotides comprising the full-length polynucleotide sequences of the novel genes and fragments thereof, the novel polypeptides encoded by the polynucleotides and fragments thereof, as well as their functional equivalents. The present invention also relates to the use of said polynucleotides and polypeptides as biotechnological tools in the production of Vitamin C from microorganisms, whereby a modification of said polynucleotides and/or encoded polypeptides has a direct or indirect impact on yield, production, and/or efficiency of production of the fermentation product in said microorganism. Also included are methods/processes of using the polynucleotides and modified polynucleotide sequences to transform host microorganisms. The invention also relates to genetically engineered microorganisms and their use for the direct production of Vitamin C.
CN102379869A Oral preparation containing saxagliptin and application thereof The invention relates to a novel oral preparation, which consists of saxagliptin of 1swung dash40mg or pharmaceutically acceptable salt and carriers thereof, wherein the oral preparation is a tablet, a capsula, a dispersible tablet, a chewable tablet, a pill, granular formulation, a dry suspension, an orally disintegrating tablet, a soft capsule, a buccal tablet, an effervescent tablet, an oral solution, an oral suspension, a drop, a sustained release preparation or a controlled release preparation, and is used for treating diabetes mellitus or related diseases. Compared with the common tablets, the dispersible tablet has the characteristics of quick and uniform dispersing, short disintegrating time, quick medicine digestion, high bioavailability, fewer adverse effects and convenience in medicine taking.
EP1534677A1 Piperidine derivatives and their use as selective inhibitors of mip-1alpha binding to its receptor ccr1 A compound of the formula (I) wherein a, b, c R1, R2, R3, R4, R5, R6, R7, Q, W, Y, and Z are defined as above , useful as potent and selective inhibitors of MIP-1α (CCL3) binding to its receptor CCR1 found on inflammatory and immunomodulatory cells (preferably leukocytes and lymphocytes).
WO2013146913A1 Hdc activation inhibitor, hdc activation inhibition composition, antipruritic agent, and antipruritic agent composition Provided are an HDC activation inhibitor and antipruritic agent effective against itching that is based on an itching-producing mechanism different from well-known itching-producing mechanisms in animals. An HDC activation inhibitor or antipruritic agent, which is one or more species selected from among (1) a specific flavonoid; (2) a tannin; (3) chlorogenic acid; (4) a specific stilbenoid, and glycosides or pharmaceutically acceptable salts of (1) to (4); or (5) a specific natural medicine extract or (6) a walnut polyphenol.
EP2598131A1 Compounds for the treatment/prevention of ocular inflammatory diseases The invention relates to the use of compounds of formula (I) and the pharmaceutically acceptable salts thereof for the treatment or the prevention of ocular inflammatory diseases, especially for the treatment and/or prevention of uveitis, severe conjunctivitis, dry eye syndrome or diabetic retinopathy.
CN101422495A Comprehensive therapy method The invention discloses an overall therapy which belongs to the field of the medical method and overcomes the defect of poor therapeutic effectiveness of traditional medical method that can only adjust a part of human body. The overall therapy is characterized by consisting of (polynutrient) food bolus (overall) and various medical methods (specialized). The overall therapy can take full consideration of point and surface, address both the symptoms and root causes, and can prevent and cure various diseases for humans more effectively.
WO2009088992A2 Ribonuclease and thiazolidinedione compounds and their use in methods to treat cancer The present invention relates to methods and kits for the treatment of cancer. A novel drug combination comprising a ribonuclease compound and a thiazolidinedione compound has been identified as producing a synergistic cytotoxicity effect in cancer cells. Methods and kits pertaining to the co-administration of these compounds are discussed herein.
CN101014610B 15beta-substituted steroids having selective estrogenic activity The invention provides 15beta-substituted steroidal compounds having selective estrogen receptor activity according to Formula (I) wherein, R<1 >is H, C1-5 alkyl, C1-12 acyl, di-(C1-5 alkyl)aminocarbonyl, (C1-5alkyl)oxycarbonyl or sulfamoyl, R<2> is H, C1-3alkyl, C2-3alkenyl or C2-3alkynyl, each of which may be optionally substituted with a halogen, R<3> is C1-2alkyl, ethenyl or ethynyl, each of which may be optionally substituted with a halogen, and R<4> is H or C1-12 acyl.
EP2686321A1 Pyrrolopyridazine jak3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
CN102302445A Clindamycin hydrochloride and sodium chloride pharmaceutical composition The invention relates to a clindamycin hydrochloride and sodium chloride pharmaceutical composition. The pharmaceutical composition is characterized by being prepared by the following pharmaceutical effective components in parts by weight: clindamycin hydrochloride, sodium chloride and appropriate amount of water for injection. By using the pharmaceutical composition, the adverse reaction caused by clindamycin hydrochloride preparation prepared in the prior art is overcome.
US20100197755 Hydrazone modulators of cannabinoid receptors Hydrazone compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
WO2013020204A1 Polymeric nanoparticles for photosensitizers Biodegradable polymeric nanoparticles comprising an inner core formed of a photodynamic agent capable of being activated to generate cytotoxic singlet oxygen are prepared. These nanoparticles have anti-cell proliferation activity and are useful in treating both cancerous and non-cancerous conditions including actinic keratosis, psoriasis and acne vulgaris. Preferably, the photodynamic agent is a hypocrellin B derivative while the polymeric nanoparticle comprises polyglycolic acid, polylactic acid or poly(lactide-co-glycolide). Hypocrellin- comprising nanoparticles are demonstrated to be activated by light or hydrogen peroxide.
CN103242315A Salt of quinoline benzamide derivative The invention relates to N-[5-(9H-purine-6-yloxy)-quinoline-8-yl]-3-(trifluoromethyl)-benzamide and a derivative fumarate or a pharmaceutically acceptable solvate thereof, and an application thereof in preparation of medicines for treating cancers.
CN102002054A Pyrazole type compound and preparation method and application thereof The invention discloses a pyrazole type compound with a structure of the formula I and a pharmaceutically acceptable salt thereof. The invention also discloses a preparation method of the compound, a medicinal composition using the compound or the pharmaceutically acceptable salt of the compound as an active ingredient, and application of the compound and the medicinal composition in preparing anantifungal medicament. The compound and the salt of the compound have a function of inhibiting fungal infections, and can be used for preparing the antifungal medicament.
US20080076811 Combinations comprising depeptidypeptidase-iv inhibitors and antidiabetic agents The invention relates to a combination which comprises a DPP-IV inhibitor and at least one further antidiabetic compound, preferably selected from the group consisting of insulin signalling pathway modulators, like inhibitors of protein tyrosine phosphatases (PTPases), non-small molecule mimetic compounds and inhibitors of glutamine-fructose-6-phosphate amidotransferase (GFAT), compounds influencing a dysregulated hepatic glucose production, like inhibitors of glucose-6-phosphatase (G6Pase), inhibitors of fructose-1,6-bisphosphatase (F-1,6-BPase), inhibitors of glycogen phosphorylase (GP), glucagon receptor antagonists and inhibitors of phosphoenolpyruvate carboxykinase (PEPCK), pyruvate dehydrogenase kinase (PDHK) inhibitors, insulin sensitivity enhancers, insulin secretion enhancers, α-glucosidase inhibitors, inhibitors of gastric emptying, insulin, and α2-adrenergic antagonists, for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of conditions mediated by dipeptidylpeptidase-IV (DPP-IV), in particular diabetes, more especially type 2 diabetes mellitus, conditions of impaired glucose tolerance (IGT), conditions of impaired fasting plasma glucose, metabolic acidosis, ketosis, arthritis, obesity and osteoporosis; and the use of such combination for the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body weight.
EP2276750A2 Substituted pyrimidines and triazines and their use in cancer therapy Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. In one embodiment, the pyrimidine and triazine derivatives are morpholino-pyrimidine, morpholino-triazine, pyridyl-pyrimidine, and pyridyl-triazine derivatives which are selective irreversible inhibitors of the p110α isoform of PI3K.
CN100998552A Composition of oral medicine preparation and its preparing method A medicinal composition for the orally taken medicines in the form of tablet, capsule, particle, micropill, dripping pill, etc contains danshinolic acid A and dashinolic acid B. Its preparing process and quality control method are also disclosed.
US7087581 Regeneration of sensitive cells with cell proliferative agents; cyclin-dependent kinase inhibitor; administering antibody In a process for the treatment of diseases or disorders of the inner ear linked with damage or destruction of sensory cells of the inner ear, for regenerating the sensory cells use is made of at least one active ingredient, which at least partly inhibits or eliminates the inhibiting action of at least one cell cycle inhibitor present in the inner ear. In this process the sensory cells of the inner ear are preferably regenerated by stimulating the proliferation of supporting cells. The sensory cells of the inner ear are so-called hair sensory cells. As cell cycle inhibitors use can be made of cyclin-dependent kinase inhibitors such as in particular the cyclin-dependent kinase inhibitor p27Kip1.
CN101311166B Tyrosine kinase restraining agent, preparation method thereof and use The invention relates to the field of pharmaceutical chemistry, in particular to a compound (I) which can treat diseases by inhibiting epidermal growth factor receptor (EGFR), that is, tyrosine kinase, prodrug of the compound, medical salt and a drug combination containing the compound. In addition, the invention also relates to a method which adopts the compound and the drug combination and can prevent, control and treat cancer by inhibiting EGFR receptor tyrosine kinase.
USRE39682 Enzyme inhibitors, for cancer therapy Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.
CN101255158B 9-N-substituted berberine derivatives as well as preparation method and use as anti-cancer drugs The invention disclose 9-N-substituted berberine derivates, a method for making same and applications as anticancer drugs, wherein the chemical formula is shown as the formula I, n is selected from 1-6; R is selected form H, amino, C1-C6 amido, hydroxyl, alkoxyl, alkoxyl, benzene ring or substituted benzene ring; m is selected from 0-1; anion X<-> is selected from halogen anion, sulfate anion, hydrogen sulfate anion, etc. the 9-N-substituted berberine derivates have strong interaction with protooncogene c-mycDNA rich in guanine, have good inhibitory activity to telomere and telomerase in cancer cells, and have strong inhibition to the expression of protooncogene c-myc. Proved by experiment, the 9-N-substituted berberine derivates of the invention have substantial inhibition to various cancer cell line, have small toxicity to normal cells, and may be used for preparing anticancer drugs. The 9-N-substituted berberine derivates of the invention has a simple preparation method, a substantial potency, and have great medicine market outlook.
CN103012291A 2-phenyl quinazoline derivative, preparation method thereof, and application in preparation of anti-cancer drugs The invention relates to the field of medicinal chemistry, in particular to a 2-phenyl quinazoline derivative. The 2-phenyl quinazoline derivative has the structural formula in the figure, wherein R1 is NH(CH2)3N(CH3)2; R2 is C1 or H; R3 is NHCO(CH2)nNR4 or NHCO(CH2)nNH(CH2)nNR4; n is equal to 1, 2, 3, 4 or 5; NR4 represents two C1-6 alkyls on an N atom, two C3-6 naphthenic bases or NR4 represents morpholinyl, piperazinyl or pyrrolidinyl. The invention further discloses a preparation of the 2-phenyl quinazoline derivative. The 2-phenyl quinazoline derivative has strong inhibition to telomere DNA expression, can significantly inhibit multiple kinds of cancer cell lines, has small toxicity to normal cells, and can be widely applied to preparation of anti-cancer drugs.
CN1582936A External used gel of Jiatishacin and its preparation An exterior-applied gel of Jiatishaxing is prepared through adding carbomer to glycerine, grinding, adding distilled water, grinding, adding the aqueous solution oftriethanolamine to obtain gel matrix, dissolving Jiatishaxing in distilled water, adding propanediol, stirring, slowly adding it to said gel matrix, adding distilled water and grinding.
CA2655759A1 Compositions and kits comprising a melatonin component and a chondroprotective component Disclosed herein are compositions and kits, wherein each composition comprises a melatonin component, a chondroprotective component, or both, and wherein each kit comprises a melatonin component and a chondroprotective component. The compositions and kits are useful for restorative sleep function and restorative joint structure or restorative joint function. Further disclosed herein are methods of using the compositions and kits.
US20120135086 Method of tissue repair using a composite material A composite biocompatible hydrogel material includes a porous polymer matrix, the polymer matrix including a plurality of pores and providing a Young's modulus of at least 10 GPa. A calcium comprising salt is disposed in at least some of the pores. The porous polymer matrix can comprise cellulose, including bacterial cellulose. The composite can be used as a bone graft material. A method of tissue repair within the body of animals includes the steps of providing a composite biocompatible hydrogel material including a porous polymer matrix, the polymer matrix including a plurality of pores and providing a Young's modulus of at least 10 GPa, and inserting the hydrogel material into cartilage or bone tissue of an animal, wherein the hydrogel material supports cell colonization in vitro for autologous cell seeding.
CN101129369A Domperidone soft capsule composition The invention belongs to the field of pharmaceutical preparation, and relates to a soft capsule preparation for promoting stomach dynamic, which is a capsule of domperidone prepared from oleic acid, linoleic acid or its esterification substance as liquid dispersion medium. The content of the preparation has better dissolvability and shorter dissolving out time.
CN101880266A Furanone compound Cytosporanone A having antibacterial activity The invention relates to the technical field of medicine, in particular to furanone compound Cytosporanone A which is separated from plant endophytic fungi Cytospora sp. leavening, has antibacterial activity and has the systematic name of (R)-5-((S)-hydroxy (phenyl)-methyl) dihydrofuran-2 (3H)-one, and the furanone compound Cytosporanone A has the chemical structural formula as follows. The in vitro antibacterial experiment proves that the compound Cytosporanone A has obvious bacteriostatic effect for botrytis cinerea, septoria musiva leaf blight fungi and bacillus megaterium, thus being used for preparing antibacterial medicines. The invention provides a lead compound for developing new antibacterial medicines, and has important valve for developing endophytic fungi medical resources of China.
CN103142603A Isoguanine compound used for treating hepatitis C virus (HCV) The invention discloses an isoguanine compound used for treating hepatitis C virus (HCV) and relates to the technical field of medicament. Isoguanine derivative (I) which has an anti-HCV activity is prepared and extracted in characteristic zhuang medicine in Guangxi called red fish eye phyllanthus reticulates. The isoguanine derivative (I) is characterized in that in a concentration range of 0Mu g/rnl-3125Mu g/rnl, the isoguanine derivative (I) has no cytotoxicity, and in a concentration range of 125Mu g/rnl-3125Mu g/rnl, the isoguanine derivative (I) has an obvious restraining effect on a replicor ribonucleic acid (RNA) of the HCV (p<0.01). The prepared isoguanine derivative (I) has broad market prospects in new drug research and development of the HCV.
WO2011074567A1 Transdermal preparation containing basic anti-inflammatory agent Disclosed is a transdermal preparation in which a basic anti-inflammatory agent is blended. The transdermal preparation is an adhesive patch for external use, which has excellent drug release properties without deteriorating the physical properties of the plaster. The transdermal preparation is capable of achieving high release properties for the basic anti-inflammatory agent without deteriorating the release properties for a local anesthetic. Specifically disclosed is an adhesive transdermal patch which is characterized by containing both a basic anti-inflammatory agent and a local anesthetic that serves as an absorption enhancer for the basic anti-inflammatory agent. The basic anti-inflammatory agent has an acid dissociation constant (pKa) of not less than 7. The basic anti-inflammatory agent is contained therein in an amount of 0.1-10% by weight relative to the total weight of the drug-containing plaster, and the absorption enhancer is contained therein in an amount of 0.01-20% by weight relative to the total weight of the drug-containing plaster.
US20140031299 Nutritional supplements and associated treatment methods A nutritional supplement, comprising a combination of resveratrol, nicotinic acid or a nicotinic acid precursor, and D-ribose in nutritionally effective amounts; and wherein the combination is configured to increase Sirtuin 1 enzymatic activity and to initiate increased NAD+ production for sustaining said Sirtuin 1 enzymatic activity. In some examples the nutritional supplement is configured to target a certain physiologic stress and is delivered in treatments including a resveratrol dose of 30 mg per day, a nicotinic acid or nicotinic acid precursor dose of 30 mg per day, and a D-ribose dose of 3 grams per day.
WO2014060493A2 N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group The present invention relates to N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
CN103040740A Ornidazole injection and preparation technology thereof The invention provides an ornidazole injection which comprises ornidazole, propylene glycol and water for injection, wherein the ornidazole can be well dissolved when the volume of the propylene glycol is 60%-70% of that of the injection. According to a preparation technology for the ornidazole injection, oxygen in the solution can be completely removed by utilizing carbon dioxide gas, and the saturated carbon dioxide gas in the injection can be used for not only reducing the oxidized by-product of the ornidazole injection, but also improving the heat stability of the ornidazole injection.
US20100254946 Maintenance of hair growth and treatment of hair-loss The present invention relates to a nucleic acid molecule, encoding a polypeptide having P2Y5 receptor function wherein said nucleic acid molecule comprises: (a) a nucleic acid molecule encoding a polypeptide having the amino acid sequence of SEQ ID NO:2; (b) a nucleic acid molecule having the DNA sequence of SEQ ID NO:1; (c) a nucleic acid molecule having the sequence of SEQ ID NO:1, wherein each thymidine is replaced by uridine; (d) a nucleic acid molecule that hybridizes under stringent conditions to the complementary strand of a nucleic acid molecule of (a), (b) or (c); (e) a nucleic acid molecule encoding a polypeptide having at least 80% sequence identity to the polypeptide of (a); or (f) a nucleic acid molecule that is degenerate with respect to the nucleic acid molecule of (b), (c) or (d); for the diagnosis, treatment and/or prevention of hair-loss and the diagnosis of a predisposition for hair-loss. Furthermore, the invention relates to compositions and uses for the diagnosis, treatment and/or prevention of hair-loss as well as to methods of identifying compounds useful in the treatment of hair-loss. The invention also relates to nucleic acid molecules carrying mutations that are causative and/or indicative of hair-loss, diagnostic compositions, kits and methods for testing for the presence of the mutant nucleic acid molecule.
WO2011110084A1 Method for preparing isovalerylspiramycin i, ii or iii and pharmaceutical composition containing compound thereof Method for preparing isovalerylspiramycin I, II or III and pharmaceutical composition containing the compound thereof which has antibacterial activity are provided. Isovalerylspiramycin I, II or III is obtained by the procedures of primary separation, high-efficient purification and post-treatment of the sample containing them. Preferably purifying the sample by HPLC to separate bitespiramycin to obtain pure isovalerylspiramycin I, II or III.
CN101292976A Medicament combination containing 1,8-eudesmin and flavanones, and uses thereof The invention discloses a drug composite containing 1, 8-cineole and blumea. The drug composite comprises the following components by weight percentage: 3.01-49.44 percent of 1, 8-cineole, 0.30-20.61 percent of sabinene, 0.60-10.30 percent of Alpha-pinene, 0.60-17.17 percent of limonene, 0.47-11.90 percent of blumea, 7.08-71.61 percent of L-borneol and 1.42-13.16 percent of Beta-caryophyllene. The drug composite has good effects on resisting the injuries of mouth, pharynx and nose caused by radiation, or curing the injurious diseases of oral cavity, throat, nose, skin and mucous and gland, can significantly reduce the suffering of patients, and provides a new choice for clinical medicine. The drug composite is safe and reliable, and is beneficial to the clinical application and acceptance of majority of patients. The invention also discloses the use of the drug composite thereof.
EP1581477B1 Cycloalkene dicarboxylic acid compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein A is a non-aromatic ring system containing 4 to 8 carbon atoms, wherein the ring system comprises at least one double bond and wherein one or more of the carbon atoms in the ring can be replaced by a group X, wherein X is selected from the group consisting of S, O, N, NR4, SO, CO or SO2; D is O, S, SO2, NR4 or CH2; Z1 and Z2 are independent from each other O, S, or NR5 ; R2 is H, OR6, or NHR7; E is an alkyl or cycloalkyl group or a monocyclic or polycyclic substituted or unsubstituted ring system which may contain one or more groups X and which contains at least one aromatic ring; Y is hydrogen, halogen, haloalkyl, haloalkyloxy, alkyl, cycloalkyl, a monocyclic or polycyclic substituted or unsubstituted ring system for the use as a medicament.
EP1137642B1 Bis-sulfonamides The invention relates to novel bis-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin antagonists.
US20110158910 Microparticles comprising polymers with thioester bonds The present invention relates to particles suitable for delivery of active agents comprising a polymer containing thioester bonds which are obtained via the reaction of a thioic acid functionality and an unsaturated group. The polymer may be is linear, branched or crosslinked. The particles have an average diameter in the range of 10 nm to 1000 μm, preferably in the range of 100 nm-100 μm. The particles may comprise an active agent selected from the group of nutrients, pharmaceuticals, proteins and peptides, vaccines, genetic materials, diagnostic agents or imaging agents. The present invention further relates to the use of the particles in dermatology, muscular skeletal, oncology, in vascular applications, in orthopaedics, in ophthamology, spinal, intestinal, pulmonary, nasal, or auricular.
US7045533 Such as naphthalen-1-yl-(4-pentyloxy-naphthalen-1-yl)-mehtane for treatment/prevention of diseases/conditions associated with cannobinoid receptor activation such as chronic pain, osteo- and rheumatoid arthritis, teno-synovitis and gout The present invention relates to novel naphthalene derivatives of formula (I), wherein R1, R2, R3 and X are as defined in the description, and preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.
EP1265615B1 Novel combination of non-sedative anti-histamines containing substances which influence the action of leukotriene, for treating rhinitis/conjunctivitis The invention relates to a pharmaceutical combination to be administered topically or orally of a non-sedative anti-histamine, with the exception of compounds of the loratadine type, and a leukotriene antagonist, selected from a leukotriene D4 antagonist, or a 5-lipoxygenase inhibitor, or a FLAP antagonist and optionally conventional, physiologically harmless supports, extenders and auxiliary agents, for the prophylaxis and treatment of allergic and/or vasomotor rhinitis or allergic conjunctivitis.
CN102058618A Emla magnesium sulfate wet dressing agent and preparation method thereof The invention discloses an Emla magnesium sulfate wet dressing agent and a preparation method thereof. The wet dressing agent is composed of 20-50% of magnesium sulfate, 0.1-4% of Emla and the balance of water for injection and medical carriers. The preparation method comprises the following steps: slicing the medical carriers and disinfecting the sliced medical carriers, and then soaking the disinfected medical carriers with an Emla magnesium sulfate solution for 30-60 minutes; and disinfecting by vapor for 30-45 minutes, then placing the disinfected medical carriers in a plastic bag and sealing to obtain the Emla magnesium sulfate wet dressing agent. The Emla magnesium sulfate wet dressing agent can effectively prevent chemotherapeutic phlebitis, and the clinical test proves that the wet dressing agent can prevent and treat swelling and pains caused by edema of local hypodermis with the treatment efficiency of over 90%, when a patient is subjected to chemotherapeutics by intravenous drip, can reach over 90%, thus relieving pains of the patient and improving the life quality of the patient.
WO2008090884A1 Novel trifluoromethylphenyltetrahydrocinnoline derivative and pharmaceutical use thereof Disclosed is a trifluoromethylphenyltetrahydrocinnoline derivative represented by the general formula (1) below or a physiologically acceptable salt thereof. The trifluoromethylphenyltetrahydrocinnoline derivative or a physiologically acceptable salt thereof has a broad antitumor spectrum against malignant tumors, and is useful as an excellent antitumor agent. (1) (In the formula, X1-X5 independently represent a hydrogen atom or a hydroxy group, and at least one of X1-X5 represents a hydroxy group; and X6 represents a hydrogen atom or a hydroxy group.)
CA2445346C N-substituted pyrazole-o-glycoside derivatives and therapeutic agent for diabetes containing the same The present invention relates to pyrazole derivatives represented by the following formulas and analogues thereof, (see formula I) (see formula II) which can be used for a therapeutic agent for diabetes.
US7342000 Semisynthetic macrolide antibiotics of the azalide series The invention relates to N″-substituted 9a-N-(N′-carbamoyl-γ-aminopropyl), 9a-N-(N′-thiocarbamoyl-γ-aminopropyl), 9a-N-[N′-β-cyanoethyl)-N′-carbamoyl-γ-aminopropyl] and 9a-N-[N′-β-cyanoethyl)-N′-thiocarbamoyl-γ-am inopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semi-synthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, R1 represents H or β-cyanoethyl moiety, R2 represents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, β-phenylethyl, ethoxycarbonyl-methyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents O and S, and their acceptable addition salts thereof with inorganic or organic acids, to the process for preparation of their pharmaceutical compositions as well as the use their compositions in the treatment of bacterial infections.
US20070254037 Methods and Compositions for the Treatment of Cell Proliferation The use of compositions which include one or more inhibitors of the citric acid, TCA, cycle and/or one or more inhibitors of oxidative phosphorylation for the treatment of cellular proliferation is disclosed. The composition is administered to or in the region of the proliferating cells or in a resection scar or cavity.
CN101550133A Method for extracting puerarin and usage of kudzu vine root for preparing medicament protecting liver The present invention discloses a methodfor extracting puerarin and an usage of kudzu vine root for preparing medicament protecting liver, the puerarin is extracted from the kudzu vine root. The method includes steps as follows: (1) comminuting and extracting; (2) concentrating; (3) upper prop; (4) eluting; (5) concentrating; (6) extracting and concentrating, finally, obtaining the coarse extract of puerarin. An animal experiment result proves that the puerarin has better effect of detoxifcation and protective liver. Compared with the prior art, the puerarin extracted by the method provided by the invention has advantages of high purity and convenient to use.
CN102659722A Amorphous cabazitaxel and preparation method thereof The invention relates to an amorphous cabazitaxel and a preparation method thereof and further relates to a medical application of a cabazitaxel amorphous substance. The amorphous cabazitaxel prepared according to the preparation method provided by the invention is low in solvent residual, is excellent in appearance form and stability and is preferably applied to clinic treatment.
CN103385872A Pharmaceutical composition for treating liver cancer and preparation method thereof The invention relates to a pharmaceutical composition for treating liver cancer and a preparation method thereof. The composition is prepared by the following medicines in parts by weight: 5-50 parts of curcumin and 0.1-10 parts of disodium cantharidinate. The composition is processed and prepared into conventional dosage forms by adding conventional auxiliary materials according to conventional technologies. The combined use of curcumin and disodium cantharidinate plays synergistic effect and has substantially better treatment effect than single use, and the composition is capable of effectively inhibiting growth of liver cancer cells and substantially alleviating pain of patients.
CN1596884A Composition containing high content conjugated linoleic acid and its preparation method A high-content conjugated linoleic acid (CLA) composition in the form of oily liquid or powder for preventing and treating obesity, diabetes and hyperlipemia is disclosed, which features high content of CLA (90-95%). It can be used also as health-care food.
US20120157442 Heteroaryl btk inhibitors The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
WO2012071684A1 Heterocyclic derivates，preparation processes and medical uses thereof Disclosed are heterocyclic derivatives, methods for making them, compositions containing the same and uses thereof. Particularly, their pharmaceutical use as inhibitors of PARP is disclosed.
WO2004096216A3 Use of a topical medicament comprising riluzole The present invention further relates to the use of Riluzole in a topical medicament for the treatment and/or prevention of neuronal or brain diseases and/or injuries, as well as topical combination preparations comprising Riluzole and agents effective in treating neuronal or brain diseases and/or injuries.
EP2350656A1 Methods and kits to identify invasive glioblastoma The invention encompasses methods and kits used in the detection of invasive glioblastoma based upon the expression of NHERF-1. The methods and kits also allow prediction of disease outcome as well as therapeutic outcome.
EP1981495A2 Use of vildagliptin for the treatment of diabetes A method for improving glucose control and for treating a patient suffering from hyperglycemia by administering the DPP-IV inhibitor vildagliptin to a patient in need thereof, before or with the- evening- meal.
EP2740475A1 Left ventricular diastolic function improving agent An agent for treating heart failure, which improves left ventricular diastolic function itself without depending on the diuretic effect or vasodilation effect; controls the pathological condition of diastolic functional failure; and prevents the recurrence, and can prevent dyspnea and death from the pathological condition, is provided. By directly acting on a heart, 4-[(2-{(2R)-2-[(1E,3S)-4-(4-fluorophenyl)-3-hydroxy-1-buten-1-yl]-5-oxo-1-pyrrolidinyl}ethyl)thio]butanoic acid improves left ventricular diastolic function, and can effectively treat diastolic functional failure among heart failure types. Accordingly, by present invention, a new agent for treating heart failure that can relieve diastolic functional failure, for which no effective therapeutic method has been established, can be provided.
WO2007119600A9 Carbazole compound The present invention provides a carbazole compound represented by formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R1 is a hydrogen atom, etc; R2 is a lower alkoxy group, etc; and R3 is a hydrogen atom, etc. The carbazole compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.
CN102626403A Disinfectant for animals and its preparation method and use The invention relates to a disinfectant for animals and its preparation method and use. The disinfectant for animals comprises a mother liquor and water, wherein the mother liquor comprises: by weight, 2.5 to 3 parts of chlorhexidine acetate, 2 to 2.5 parts of benzalkonium bromide, 1.2 to 1.7 parts of triton and 1.2 to 1.7 parts of glutaraldehyde. The preparation method comprises the following steps of mixing chlorhexidine acetate, benzalkonium bromide and glutaraldehyde of the mother liquor at a normal temperature, adding water into the mother liquor to obtain a mixed solution, wherein the weight of the water is 3 times of the total weight of chlorhexidine acetate, benzalkonium bromide and glutaraldehyde, cooling the mixed solution to a temperature of -5 DEG C, keeping the temperature for 8 hours, gradually heating the mixed solution to a temperature more than 50 DEG C, adding triton into the mixed solution while heating the mixed solution to a temperature of 90 to 100 DEG C so that triton is completely dissolved in the mixed solution, then adding water into the mixed solution containing triton, and cooling to a normal temperature to obtain the disinfectant for animals. The disinfectant for animals can be used for fed animals and aquatic products and has strong bactericidal power, a wide antimicrobial spectrum, wide purposes, stable performances, high use safety, short onset time and long sterilization lasting time.
CN101084896A Atracurium freezing-dried composition The invention discloses freeze drying composition of atracurium. The composition adopts atracurium or its pharmaceutically acceptable salt or optical isomer as active ingredient, and also comprises sugar and organic acid. The invention also discloses a method for preparing the composition. The inventive composition has good water-solubility and good storing stability, low stimulation to blood vessel, and high safety; is suitable for clinical application.
CA2675981A1 Thiophene derivatives useful as ocular hypotensive agents Disclosed herein is a compound of the formula. Therapeutic methods, compositions, and medicaments for the treatment of glaucoma or ocular hypertension related thereto are also disclosed.
US20130251814 Magnetic nanodrug for treating thrombosis The present invention discloses a magnetic nanodrug for treating thrombosis, which comprises a core formed of magnetic nanoparticles, a shell enveloping the core and made of carboxyl-functionalized polyaniline, and a thrombosis-treatment drug covalently bonded to the shell. The magnetic nanodrug of the present invention is non-toxic to vascular endothelial cells, has superior stability, features superparamagnetism, and can be uniformly dissolved in water. Therefore, the magnetic nanodrug for treating thrombosis can be guided by an external magnetic field to concentrate on a specified region and increase the effect of thrombosis treatment.
CA2747252A1 Pyrazine derivatives useful as inhibitors of atr kinase The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; pro-cesses for preparing the compounds of this invention; in-termediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The com-pounds of this invention have formula (I):wherein the variables are as defined herein.
CN103145736A Medicine composite containing cefamandole nafate compound The invention discloses a cefamandole nafate compound for injection. The cefamandole nafate compound is a crystal compound; and in X-ray powder diffraction, main peaks are shown at diffraction angles of 5.9+/-0.01 degrees, 6.02+/-0.01 degrees, 11.3+/-0.01 degrees, 16.9+/-0.01 degrees, 17.9+/-0.01 degrees, 18.0+/-0.01 degrees, 21.1+/-0.01 degrees, 22.0+/-0.01 degrees, 22.1+/-0.01 degrees, and 23.5+/-0.01 degrees. The invention also discloses a medicine composite containing the cefamandole nafate compound. The cefamandole nafate crystal is good in stability and high in fluidity; when a cefamandole nafate sterile powder injection is prepared, the sub-package amount of active medicine components is accurate and the operation is facilitated; and besides, the sterile powder injection is not easily adhered to bottles, and is very convenient regardless of being used independently or mixed with other medicine powder. The cefamandole nafate compound does not degrade fundamentally and can be placed for a long time, thereby having a great advantage in medicine preparation.
US20070286901 Novel Pharmaceutical Formulation of Cefixime for Enhanced Bioavailability A chewable tablet comprising Cefixime having a mean particle size between 20 μ and 120 μ wherein the said composition demonstrates bioequivalence to a suspension of Cefixime trihydrate. The process of preparation of the chewable tablet comprises the steps of optionally micronizing Cefixime such that the mean particle size of the Cefixime particles is between 20 μ and 120 μ, blending with other excipients, roll compaction, milling to form granules, blending to form a secondary blend and compression of the secondary blend to form tablets.
WO2006116815A1 Composition for the control of cholesterol levels The present invention relates to a composition used to control cholesterol levels. In particular, the present invention relates to a method for the treatment or prevention of disorders or diseases mediated by hyperlipidemia, said method comprising administering to a mammalian subject in need thereof an effective amount of a composition comprising an extract from at least one plant from the genus Stevia and at least one bile salt, salt thereof or derivative thereof admixed in a form suitable for therapeutic administration.
WO2009137916A1 Processes and intermediates for the preparation of oseltamivir and analogs thereof The present application relates to processes for the preparation of oseltamivir and the H3PO4 salt of oseltamivir, Tamiflu®. The application further relates to novel intermediate compounds and to pharmaceutical compositions containing said compounds. The application further relates to a method of using the novel intermediates to treat or prevent influenza.
US20050095239 Methods and compositions for treating Alzheimer's disease The present invention provides methods for reducing the efflux of cholesterol and/or secreted Aβ in the brain, as well as methods for treating Alzheimer's disease, by inhibit the expression and/or activity of LXR and/or ABCA1. Compositions comprising agents for performing the methods also are provided.
WO2007017577A1 7-substituted aza-indazoles, compositions containing same, production method and use thereof The invention relates to specific novel 7-aza-indazoles having formula (I), which modulate the activity of proteins, particularly kinases, compositions containing same and the use thereof as a medicament, in particular as anticancer agents.
CN101756937A Combined capsule with replaglinide solid preparation and dimethyldiguanide solid preparation The invention relates to a combined capsule filled with a replaglinide solid preparation and a dimethyldiguanide solid preparation. The combined capsule comprises a first capsule and a solid preparation in the first capsule, wherein the first capsule comprises an upper capsule body and a lower capsule body; and the solid preparation with an active component of replaglinide and the solid preparation with an active component of dimethyldiguanide are at least filled into the first capsule. Compared with the prior art, all components can not generate chemical change and produce a by-product so that the stability of a product is improved. The product of the invention is quite suitable for industrialized production and has favorable compliance of patients.
EP2209777A2 Thiazol derivatives for treating cancer The invention relates to compounds of formula (I), in which R1, R2, R3, R4, K, G, E and W can be defined as cited in claim 1. Said compounds are used for treating tumours.
CN103585416A Drug composition for treating herpes zoster The invention discloses a drug composition for treating herpes zoster, and belongs to the technical field of drug compositions. The drug composition comprises the following raw materials: radices trichosanthis, roots of common peony, cape jasmine, scutellaria baicalensis, golden cypress, rheum officinale, angelica, indigo naturalis, dried orange peels, radix angelicae, felwort, fructus forsythiae, gallnuts, monkshood, borneol, realgar, alum, coptis chinensis, centipedes, myrrh, peppers, paris polyphylla, pedate pinallia jackinthepulpit rhizome, pinellia ternate and honey. The drug composition is reasonable in drug compatibility, the effects of clearing heat, promoting diuresis, soothing liver-gallbladder, removing toxins and blood stasis, activating meridians to stop pain, tonifying the spleen and eliminating moisture are used as treatment principles, the herpes zoster can be effectively treated, and pain of patients is relieved.
CN103202820A Stable enteric lansoprazole capsule and preparation method thereof The invention discloses a stable enteric lansoprazole capsule prepared through a nanometer technology, and a preparation method thereof. The capsule is composed of the following components, by weight, 1.0 part of lansoprazole (having a raw material particle size of 400-500nm), 0.67-3.0 parts of mannitol, 0.67-2.0 parts of talcum powder, 0.1-0.3 parts of starch, 0.03-0.1 parts of disodium hydrogen phosphate, 0.03-0.1 parts of hydroxypropyl methyl cellulose, 1.0-1.5 parts of polyvinylpyrrolidone K, 6.0-9.0 parts of 95% ethanol, 2.0-3.0 parts of acrylic resin II, 0.08-0.12 parts of diethyl phthalate and 0.03-0.05 parts of polysorbate 80. In the above preparation, mannitol and the talcum powder are used as diluents, and disodium hydrogen phosphate is used as a pH value adjusting agent to make the core of a pellet alkaline and improve the stability of lansoprazole; and the quality of the enteric lansoprazole pellet capsule prepared through adopting the preparation method is reliable, and reaches English BP standards.
WO2009023180A1 SUBSTITUTED BICYCLIC PIPERIDINYL-AND PIPERAZINYL- SULFONAMIDES USEFUL TO INHIBIT 11β-HYDROXYSTEROID DEHYDROGENASE TYPE-1 In its many embodiments, the present invention relates to a novel class of substituted bicyclic piperidinyl- and piperazinylsulfonamide compounds useful to inhibit 11β-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11β-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
US20050002970 Enhancing flowability and lubricity; artificial tears, ocular lubricants The use of nanoparticles of inorganic materials (e.g., synthetic smectite clays) in ophthalmic and otic pharmaceutical nanoparticles are utilized to modify the rheological properties of the compositions, so as to enhance the viscosity, flow characteristics, lubricity or other characteristics of the compositions. The invention is particularly directed to the provision of lubricant compositions for the eye and ear, and to enhancement of the viscosity, shear thinning and lubricity of artificial tear compositions.
CN103193668A Chiral indan derivant and preparation method and application thereof The invention discloses a chiral indan derivant shown in a general formula I and pharmaceutically acceptable salts, and a preparation method and application of the chiral indan derivant. In a general formula I, X represents carbonyl, CH2, CHR4, C=CHR4, CR4R5, naphthenic base or imidazolidines substituted naphthenic base, wherein R4 and R5 represent hydrogen atoms or alkyl; R1 represents selectable substituted alkyl, selectable substituted amino or selectable substituted imidazolidines group; R2 represents hydrogen atoms, selectable substituted alkyl or selectable substituted imidazolidines group; and R3 represents hydrogen atoms or selectable substituted alkyl, benzyl or benzyl in which aromatic rings are substituted. The compound is high in melatonin acceptors MT1 and MT2 which are used for exciting the activity, can be applied to preparation of medicines for resisting insomnia and depression, and can be clinically used in modes of oral administration, intravenous injection, intramuscular injection and the like.
WO2009097414A1 Use of imidazolylalkyl-pyridines for the treatment of addictive disorders The present invention relates to the use of certain azolylalkyl-pyridines to treat addictive disorders, psychoactive substance use disorders, intoxication disorders, inhalation disorders, alcohol addiction, tobacco addiction, and/or nicotine addiction.
CN1857291A Externally applied liquid asiaticoside preparation and its preparing process The externally applied liquid asiaticoside preparation has effective component comprising asiaticoside 0.1-30.0 wt% and medicinal solvent 70.0-99.9 wt%. Its preparation process includes dissolving asiaticoside in the medicinal solvent, filtering, filling, sterilizing and packing. The present invention expands the clinical application of asiaticoside, and the abacterial preparation has high medicine concentration, high medicinal effect, no wound infection, and other advantages.
US20110038949 Homeopathic formulation The present invention relates to homeopathic formulations comprising at least Causticum, Natrium muriaticum and a Solanaceae (e.g. Datura or Hyoscyamus); said formulations are useful for treating neurological disorders.
CN103040862A Drug for treating epidemic parotitis The invention relates to a drug for treating epidemic parotitis. The drug is prepared from the following active pharmaceutical ingredients: 30-100 parts of mercury, 18-28 parts of red lead, 10-30 parts of alumen, 10-18 parts of potassium nitrate, 10-18 parts of melanterite, 6-12 parts of arsenic and 9-12 parts of native copper. The drug is reasonable in formula, has an exact curate effect and can effectively treat epidemic parotitis.
CN101837118B Compound chicken colibacillosis resisting veterinary drug preparation The invention belongs to a chicken colibacillosis controlling composite in a veterinary drug, which mainly comprises the following components in percentage by weight: 10% of florfenicol, 5% of colistin sulfate, 40% of dextrin and the balance of jiayi powder. The veterinary drug composition is used for treating chicken colibacillosis. The composition has the processing technology that each effective component is accurately weighed according to weight proportion after being dried, the florfenicol is firstly added to be mixed with cosolvent for 10 min, then other components are added for mixing for 20 min, semi-finished products are detected for the quality, sub-packaged and packaged, and the finished products are detected for the quality and put in storage. The use method is that the composition is taken with water in the proportion of 0.1%, and continuous 3-5 days is one course of treatment. The invention has high sensitivity on the chicken colibacillosis, has good effect and low drug resistance, is used conveniently, and has good popularization and application values.
WO2006064339A1 Chromane derivatives useful as acid pump antagonists This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R', R2, R3, R4, R5, R6, R7, R8 A and B are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zollinger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.
CA2809606A1 Compositions and methods for treating bone defects A bone graft composition includes a biologically-resorbable cement and a plurality of processed bone particles, where each of the bone particles have a shape configured to interconnect with adjacent bone particles. A method for treating a bone defect using the bone graft compositions includes providing the bone graft composition and administering an effective amount of the bone graft composition to a site of a bone defect in a subject. Kits including a biologically-resorbable cement powder and a plurality of processed bone particles are also provided.
WO2008015516A1 Fused tricyclic heterocycles for the treatment of schizophrenia Disclosed are compounds of Formula (1), pharmaceutical compositions containing compounds of Formula (1), and the use of compounds of Formula (1) to treat central nervous system disorders, including schizophrenia and other psychotic disorders, wherein L, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 R8, R9 and R10 in Formula (1) are defined in the specification.
EP1497672A2 Ultrasonic doppler effect speed measurement An ultrasound transducer (12) is coupled to a transmitter (11) having a source of ultrasound signal. A receiving ultrasound transducer (13) is coupled to a preamplifier (14) and mixer (15). The mixer (15) is further coupled to a demodulator (16) and filter (17) which in turn is coupled to an amplifier (18) and a comparator (19). The comparator (19) output is coupled to a controller (20) which performs edge detection of the comparator output signal. The transmitter (11) produces ultrasound energy which is reflected from an object (31) to the receiving transducer (13). The shift in frequency between the transmitted ultrasound energy (30) and the reflected ultrasound energy (32) is used to determine the speed of the object (31) by employing Doppler effect. Frequency detection is enhanced by mixing the transmitted and reflected ultrasound signals to provide a beat frequency signal.
US20090258426 Preferred segments of neural thread protein and method of using the same The invention is directed to preferred repeat sequences of Neural Thread Protein (NTP), peptides, mimetics, antibodies, and nucleic acids of the preferred sequences, and diagnostic and therapeutic methods of using such preferred NTP sequences.
US20110229457 Injectable drug delivery system The invention provides a formulation that includes a biocompatible solvent system, a biodegradable polymer that is substantially soluble in the biocompatible solvent system, and an active pharmaceutical ingredient that is substantially insoluble in the biocompatible solvent system. The formulation can form a drug-eluting implant, when injected into mammalian tissue. The solvent system and the biodegradable polymer can be selected so that the implant provides extended, delayed, controlled and/or modified release of the active pharmaceutical ingredient, for example, over the course of days, weeks or months.
CN103360342A 3-Cyanoaniline alkyl aryl piperazine derivative and application in preparing medicaments The invention discloses a 3-cyanoaniline alkyl aryl piperazine derivative and application thereof in preparing medicaments. The 3-cyanoaniline alkyl aryl piperazine derivative disclosed by the invention has very useful pharmaceutical properties and excellent tolerance, and especially can be used as a novel analgesia, a novel antidepressant medicament, and a novel analgesic and antidepressant medicament. The compounds are 5-hydroxytryptamine regulated central analgesias, and also are 5-hydroxytryptamine regulated novel antidepressant medicaments. The compounds also are low in toxic and side effects and large in safety range. The 3-cyanoaniline alkyl aryl piperazine derivatives are compounds as shown in a formula (III), or free bases or salts thereof.
WO2007082909A3 Method for treating huntington's disease by inhibiting dephosphorylation of huntingtin at s421 The present invention relates to a method for treating patients having Huntington's disease by a drug increasing the phosphorylation of huntingtin at position 5 S421, thereby decreasing the polyQ-huntingtin-induced toxicity. Useful compounds are selected from the group consisting of cyclosporin A, FK506, FK520, L685,818, FK523, 15-0-DeMe- FK520, Lie120, fenvalerate, resmethrin, cypermethrin, deltamethrin. A method for selecting, identifying or screening a compound useful for treating a subject having Huntington's disease is also disclosed.
WO2007054954A1 A novel pyrrolo[2,1-c][1,4]benzodiazepine hybrid and a process for the preparation thereof The present invention provides novel pyrrolo [2,1-c][1,4]benzodiazepine hybrid. This invention also provides a process for the preparation of novel pyrrolo[2,1-c][1,4] benzodiazepine hybrid. These novel pyrrolo [2,1-c][1,4]benzodiazepine hybrid are useful as antitumour agents. More particularly, it provides a process for the preparation of 7-methoxy-8-{n-[4-(2-oxo-2H-4-chromenyl)piperazino]alkyl}-oxy-(11aS)-1,2,3,11a-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one and 7-methoxy-8-{n-[4-(7-alkoxy-8-methyl-2-oxo-2H-4-chromenyl)piperazino]alkyl}-oxy-(11aS)-1,2,3,11a-5H-pyrrolo[2,1-c][1,4]. benzodiazepine-5-one with aliphatic chain length variations for these compounds.
CN102697780A Compound simvastatin nicotinate sustained-release capsules and preparation method thereof The invention discloses a method for preparing compound simvastatin nicotinate sustained-release capsules, and belongs to the field of medicinal preparations. Components of the simvastatin nicotinate sustained-release capsules can exert a synergistic effect in vitro and comprehensively regulate the components of blood fat, so that the medicinal effect is furthest exerted, the toxic or side effect of the medicament can be reduced, fluctuation of blood concentration in vitro is reduced, and the administration frequency of a patient is reduced; and by designing pellets, the contact area between the medicament and the digestive tract is greatly improved, and the bioavailability of the medicament is improved. The method is strong in specificity, good in reproducibility, high in precision and convenient to operate; the capsules can be well applied to treatment of hyperlipidemia and abnormal mixed blood fat; and safety, effectiveness and controllability of clinical medication are really ensured.
CA2555367A1 Apoe genetic markers associated with age of onset of alzheimer's disease Haplotypes in the APOE gene associated with age of onset of Alzheimer~s Disease are disclosed. Compositions and methods for detecting and using these APOE haplotypes in a variety of clinical applications are disclosed. Such applications include articles of manufacture comprising compounds effective in delaying the age of onset of AD in individuals at risk for developing AD and having one of these APOE haplotypes, methods and kits for predicting the age of onset of AD in an individual at risk for developing AD based upon his/her haplotype profile, and methods for delaying the age of onset of AD in individuals at risk for developing AD based upon their haplotype profile.
EP1507519A1 Medicament with delayed release of the active substance, containing 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol The invention relates to a pharmaceutical formulation with delayed release of the agent, containing 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol or one of the pharmaceutically acceptable salts thereof in a matrix. Said matrix contains 1 to 80 percent by weight of one or several hydrophilic or hydrophobic polymer/s as pharmaceutically acceptable matrix-forming substance/s and has the following dissolution rate: 3-35 percent by weight (relative to 100 percent by weight of active substance) of 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol are released after 0.5 hours; 5-50 percent by weight of % 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol are released after 1 hour; 10-75 percent by weight of 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol are released after 2 hours; 15-82 percent by weight of 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol are released after 3 hours; 30-97 percent by weight of 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol are released after 6 hours; more than 50 percent by weight of 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol are released after 12 hours; more than 70 percent by weight of 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol are released after 18 hours; more than 80 percent by weight of 1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol are released after 24 hours.
WO2012135166A1 (fused ring arylamino and heterocyclylamino) pyrimidynyl and 1,3,5-triazinyl benzimidazoles, pharmaceutical compositions thereof, and their use in treating proliferative diseases Provided herein are (fused ring arylamino and heterocyclylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula (I), and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.
US20080095810 Nanoparticle systems for release of biologically active molecules formed by chitosan polymer or derivatives, chemically modified with polyethylene glycol and crosslinked with a crosslinking agent; especially useful for pharmaceutical compositions, vaccines and cosmetic formulations; controlled release The present invention relates to nanoparticle systems for the release of biologically active molecules formed by the chitosan polymer or its derivatives, chemically modified with polyethylene glycol and crosslinked with a crosslinking agent. These systems are especially useful for pharmaceutical compositions, vaccines and cosmetic formulations.
CN101112410A Composition of indigo fruit, isoflavone and calcium The present invention relates to a food or drug which is prepared by the composition of lonicera caerulea var. edulis and isoflavones with the calcium compatibility. The present invention is in line with the theory of anti-oxidation and calcium supplement and combines the lonicera caerulea var. edulis, isoflavones which have a variety of rich natural nutrients and calcium carbonate scientifically, thus supplementing a variety of natural nutrients comprehensively, at the same time, the high efficient anti-oxidation can prevent and treat a variety of aging diseases, and the high efficient calcium supplement can also prevent and treat the bone diseases of osteoporosis. As the lonicera caerulea var. edulis and isoflavones have the special effects of skin care, anti-endometritis and so on, the invention is especially applicable for women to use.
CN103127135A Triterpene derivative and preparation method and application The invention relates to one type of triterpene, a derivative of the triterpene, a preparation method of the triterpene and the derivative of the triterpene, application in prevention and treatment of viral hepatitis and in particular to the application in treatment and prevention of viral hepatitis C. The triterpene and the derivative of the triterpene are compounds or salts or aquo-complexes of the salts like a structural formula 1 and a structural formula 2 expressed by an instruction book, wherein, the salts or aquo-complexes of the salts can be accepted in pharmacy. A substituent group and symbols are showed in definition of the instruction book.
US20110160166 Therapeutic composition for the treatment and prevention of athlete's foot and fungal infections of the nail and surrounding tissues Methods and topical pharmaceutical formulations are provided for the treatment of athlete's foot (tinea pedis) and nail fungus (onychomycosis). The invention involves an anhydrous composition containing a therapeutically effective amount of salicylic acid. Repeated applications of the resulting formula over a 4-12 week period resolve most infections without the use of systemic drugs.
US20090239874 Pyrido[3,2-e]pyrazines, their use as inhibitors of phospohodiesterase 10, and processes for preparing them The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms.
CN101337957A Scutellarin derivates, preparation method and application thereof The invention relates to a novel scutellarin derivant (1), a preparation method and the application thereof. A pharmacological experiment proves that the compounds have obvious antineoplastic activity and can be used for preparing antitumor drugs.
CN101732274A Colchicine bilayer sustained-release tablet and preparing method thereof The invention discloses a colchicine bilayer sustained-release tablet which comprises a quick release layer and a sustained-release layer, wherein the quick release layer mainly consists of colchicine, a disintegrant, a filler, a lubricant and an adhesive; the sustained-release tablet mainly consists of colchicine, a sustained-release matrix, a retarding agent, a filler and an adhesive; the weight ratio of the colchicine in the quick release layer to the colchicine in the sustained-release layer is (0.25-0.42) : 1; and the weight ratio of the quick release layer to the sustained-release layer is 1: 2 to 1: 4. The invention also discloses a method for preparing the colchicine bilayer sustained-release tablet. The colchicine bilayer sustained-release tablet releases the drugs through the quick release layer to quickly achieve the effective blood drug concentration, slowly releases the drugs through the sustained-release layer to exert and sustain the stable and uniform effective blood drug concentration, reduces the drug taking times and lightens the toxic or side function.
EP2279727A2 Nanoparticulate aripiprazole formulations The present invention is directed to compositions and methods comprising nanoparticulate aripiprazole, or salts or derivatives thereof, having improved bioavailability, faster rates of absorption and a faster onset of therapeutic effect. The nanoparticulate aripiprazole compositions are proposed to have an average effective particle size of less than about 2000 nm, and may be useful for the treatment of diseases and disorders of the central nervous system, including mental diseases and disorders.
CN1813752A Fluorouracial nano particle formulation and its preparing method The present invention relates to a new dosage form of antineoplastic fluorouracil-nano particle preparation and its preparation method. Said invention adopts chitosan-polyacrylic acid nano particles as carrier, so that it has good biological compatibility and adhesion property, the grain size of the nano particle is 50-250 nm. Said fluorourocil can be made into nano particle dry powder preparation.
US20050070487 Composition, formulations and kit for treatment of respiratory and lung disease with non-glucocorticoid steroids and/or ubiquinone and a bronchodilating agent A pharmaceutical or veterinary composition, comprises a first active agent selected from a non-glucocorticoid steroid or analogues, a ubiquinone, or salts thereof, and a second active agent comprising a bronchodilator. The composition is provided in various formulations and in the form of a kit The products of this patent are applied to the prophylaxis and treatment of respiratory, lung and malignant diseases.
US7776879 anticholinergic agents such as Butylthiophen-2-ylmethylcarbamic acid 1-azabicyclo[2.2.2]oct-3-(R)yl ester, having a high affinity for muscarinic M3 receptors, useful for treating respiratory system, urogenital, gastrointestinal and cardiovascular disorders A carbamate of formula (I), wherein R1 represents wherein R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 or 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicylic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof. The pharmaceutically acceptable salt may be of formula (II).
CN101780085A Cefprozil medicinal composition The invention relates to a cefprozil medicinal composition, in particular to a medicinal composition containing cefprozil and cellulose derivatives, which is prepared by a dry granulation method. The cefprozil and the cellulose derivatives are uniformly mixed, and the mixture is pressed into plates under the pressure of 0.1 to 25MPa so as to form tight combination; and then, according to requirements, the plates are prepared into tablets, powder, granules or capsules. The medicinal composition can further contain other conventional auxiliary materials; the obtained plates are ground, mixed with a diluent, a disintegrating agent, a lubricating agent, an adhesive and/or other auxiliary materials; and the mixture is prepared into tablets, powder, granules, suspension or capsules according to requirements. The dry granulation process is adopted; and after the cefprozil and the cellulose derivatives are tightly combined through proper pressure, the beta-lactam ring of the cefprozil is effectively prevented from ring-opening degradation, the stability of the medicinal composition is improved, and the effectiveness and safety of clinical medication are further guaranteed.
US20080069827 miRNA of HSV-LAT and uses thereof This invention relates to treatment of Herpes Symplex Virus infection. Specifically, the invention relates to the use of a newly discovered miRNA in the silencing of HSV-LAT gene, which is responsible for the prevention of apoptosis of infected neuronal cells and the maintenance of latency.
US20130029990 Pyrazole p38 map kinase inhibitors There are provided inter alia compounds of formula (I): wherein R1, R2a, R2b, R3, R4, L, X, R5 and R6 are as defined in the description for use in the treatment of inflammatory diseases.
CN1927815A Compound of o-benzylamino phenyl ether, derivative, preparation method and use of the same The present invention discloses one kind of o-benzyl amido ether compound and its preparation process and phenol derivative, as well as two preparation processes of the phenol derivative. The o-benzyl amido ether compound and its phenol derivative the present invention designs have specific pathogenic bacteria inhibiting and killing effect, and may be used as disinfectant, disinfectant precursor, biopreparate material for sterilizing, deodorizing, etc.
CN103505409A 3-n-butylphthalide injection and preparation method thereof The invention relates to a 3-n-butylphthalide injection and a preparation method thereof. The 3-n-butylphthalide injection disclosed by the invention comprises 3-n-butylphthalide or a derivant thereof, a surfactant and water for injection, wherein the surfactant is selected from one or more of phospholipid, polyethylene glycol-12-hydroxy stearate, polyethylene glycol-VE (Vinyl Ether) carbonic ester, polyethylene glycol-VE succinate, polyethylene glycol-DSPE (distearoyl phosphoethanolamine), polyethylene glycol-cholesteryl hemisuccinate, polyethylene glycol-cholesterol methyl ester, polyethylene glycol-cholesterol sulfate, polyoxyethylene dehydration sorbitol fatty acid ester and poloxamer. By adopting the 3-n-butylphthalide injection disclosed by the invention, a special fragrance of the 3-n-butylphthalide can be effectively concealed; the 3-n-butylphthalide injection is stable in quality, high in 3-n-butylphthalide content, simple in preparation technology, strong in operability and beneficial to industrialization, can be separately subpackaged into small volume of preparation, can be applied to intravenous injection, and also can be applied to intramuscular injection; the clinical drug delivery requirements are met.
CN101040848B Method for preparing amphiphilic nanoparticles The invention relates to a method for preparing amphipathic polymer carrier nanometer particle, belonging to nanometer drug technique. The invention comprises that respectively dissolving amphipathicpolyether and hydrophobic drug into organic solvents, adding the solution with amphipathic polyether into 1000 times of deionized water, mixing via magnetic force for 0.5-3h, dropping the solution with drug into the system, mixing via magnetic force for 1-4h at room temperature, evaporating out the organic solvent, freezing and drying to obtain the amphipathic polymer carrier nanometer particle. The invention has simple process, uniform grain diameter, narrow graininess distribution, high carrier and packing rate on hydrophobic drug. The invention improves the carrier and packing rate of nanometer particles, and controls the instant release condition of hydrophobic drug.
US20100263066 Inert dna sequences for efficient viral packaging and methods of use The instant invention provides an inert DNA sequence having a length of between about 0.5 kb and about 5 kb, wherein said isolated inert DNA sequence does not contain an open reading frame and which is suitable for efficient packaging of expression cassettes comprising a nucleic sequence encoding a therapeutic agent into viral vectors, as well as methods of selecting such inert DNA sequences. The invention also provides DNA constructs and medical composition comprising such inert DNA sequences, and kits and medical systems for delivering such DNA constructs and/or compositions.
US20100266588 Breast Cancer Susceptibility Gene GT198 and Uses Thereof It has been discovered that the human GT198 gene (gene symbol PSMC3IP) at chromosome 17q21 acts as a tumor suppressor. The mutation of the GT198 gene causes the increased dominant negative splice variant activity and leads to the loss of wild type GT198 function, and in turn, induces breast and ovarian cancers. One embodiment provides compositions and methods for treating or alleviating one or more symptoms associated with cancer due to the GT198 gene mutations. Another embodiment provides methods and compositions for detecting cancer due to the mutation of the GT198 gene. Still another embodiment provides methods for identifying compounds, antibodies and natural product molecules that are useful for treating cancer due to the mutations of the GT198 gene. Preferably the disclosed compositions antagonize or interfere with the biological activity of splice variants of GT198.
US20110064788 Pharmaceutical compositions for treatment of addiction The invention provides transdermal patches comprising an adhesive and a composition comprising naltrexone and either methyl oleate or isopropyl myristate, a kit comprising a plurality of such transdermal patches, a composition comprising naltrexone and methyl oleate, such a composition for use as a medicament, and compositions comprising naltrexone and methyl oleate or isopropyl myristate for use in the treatment of alcoholism or opiate addiction.
CN1947751A External application medicated bag for treating anhypnia and its prepn. method An exterior-applied medicinal bag for treating insomnia by applying it onto Shenque acupoint is prepared from the Chinese-medicinal materials through pulverizing, mixing, loading the mixture in cloth bag, and sealing.
WO2007107285A1 Lipid a antagonists with anti-septic shock, anti-inflammatory, anti-ischemia and analgesic activity The present invention relates to compounds of general formula (I), wherein R1-R4 are as defined in the description, to processes for their preparation and to their use as medicaments. The compounds of formula (I) inhibit the effect of lipid A on the Toll-like Receptor 4 and are endowed with anti-septic shock, anti-inflammatory, anti-ischemia and analgesic activity.
WO2007005951A2 Stereoisomeric pyridyl and pyridonyl compounds and methods for the treatment of gastrointestinal and central nervous system disorders The subject invention provides stereoisomeric compounds of formulae (Xa) and (Xb); wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.
WO2007111983A3 New therapeutic combinations for the treatment or prevention of psychotic disorders Therapeutic combinations useful in the treatment or prevention of psychotic disorders, to pharmaceutical compositions containing said combinations, and to their use in the treatment or prophylaxis of psychotic disorders are provided. Such compounds are of formula (I) or a pharmaceutically acceptable salt thereof, wherein each of R1, R2, R3, R4, R5, R6, n, and m are as defined and described herein.
WO2014122303A1 Glucan synthase inhibitors The present invention provides compounds with anti-fungal activity useful for treatment or prevention of fungal infections in human beings or plants. The antifungal compounds are inhibitors of glucan synthase and have the formula (I) (I) wherein Z denotes a mono- or bicyclic aromatic or heteroaromatic ring system; and X1 and X3 are individually selected from the group consisting of -CH and N, wherein at least one of X1 and X3 is N; and X2 is selected from the group consisting of –CH2, -CH-R8 and –(C=O), wherein R8 is C1-3 alkyl; and Y is selected from the group consisting of –(CH2)n-, -(CHR9)-, -(CH2)p-CR10R11- (CH2)q, -(CH2)p-(C=O)-(CH2)q and -(CH2)p-(C=O)-(CH2)q, wherein n is an integer in the range of 1 to 6, p is an integer in the range of 0 to 3 and q is an integer in the range of 1 to 4 and wherein R9 R10 and R11 individually are selected from the group consisting of C1-3-alkyl; and R1 and R5 are individually selected from the group consisting of –H and halogen, wherein at least one of R1 and R5 is halogen; and R2 and R4 is selected from the group consisting of –H and halogen; and R3 is –NH-R6, wherein R6 is selected from the group consisting of –H, alkyl, - (C=O)-R7, -(C=O)-O-R7, - (C=O)-NH2 and –SO2-R7, wherein R7 is selected from the group consisting of –H and alkyl, or a pharmaceutically acceptable salt thereof or a prodrug thereof.
CA2494302C Acylated, heteroaryl-condensed cycloalkenylamines and their use as pharmaceuticals The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines of the formula I, (I) in which A, R1, R2, R3, R4, R5 and n have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds which are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (NO) synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
US20120022037 Aqueous hair cleansing agent The present invention relates to an aqueous hair cleansing agent which includes the following components (A), (B): (A) sulfate-type anionic surfactant having a specific structure, (B) polyoxyethylene alkyl ether-type nonionic surfactant having a specific structure, and water, wherein ratio of weight represented by (B)/((A)+(B)) is 1% to 25%.
CN103330916A Blood activating and stasis dissolving cream and preparation method thereof The invention relates to a blood activating and stasis dissolving cream and a preparation method thereof. The blood activating and stasis dissolving cream comprises the following components in parts by weight: 5-10 parts of frankincense, 4-8 parts of myrrh, 4-7 parts of radix aconite, 4-10 parts of sanguis draconis, 1-6 parts of fineleaf schizonepeta herb, 3-7 parts of tortoise plastron, 1.5-3 parts of asarum sieboldii, 3-8 parts of wood puerarin, 4-8 parts of turmeric, 6-13 parts of radix angelicae, 4-6 parts of cortex phellodendri, 2-5 parts of turpentine, 3-6 parts of methyl salicylate, 113.4-290.8 parts of yellow lead and 261-569.1 parts of almond oil. The blood activating and stasis dissolving cream provided by the invention has common curative effects for symptom of sore pain and extravasated blood caused by unknown reasons, and is effective in treatment and takes effect quickly.
EP1227810B1 Treating cancer by increasing intracellular malonyl coa levels A method of killing cancer cells by acute elevation of cellular malonyl Coenzyme A (Malonyl CoA) which leads to apoptosis. Elevation of malonyl CoA may be induced by inhibition of fatty acid synthase (FAS), or by other manipulation of fatty acid metabolism. Alternatively, growth of tumor cells may be inhibited by FAS inhibition in conjunction with inhibition of carnitine palmitoyltransferase-1 (CPT-1). Combination therapy with drug(s) that inhibit fatty acid synthesis by inhibiting acetyl CoA carboxylase (the first enzyme in the fatty acid synthesis pathway) and drug(s) that inhibit CPT-1 e.g. etomoxir may be expected to induce apopptosis in tumor cells.
CN1618430A Adefovir composite medicine for treating hepatitis B A medicine for the form of capsule, tablet, or particles for treating hepatitis B is prepared from adefovirdipivoxil ester, one of rheum emodin, matrine oxide, the extract of astragalus root, notoginseng, etc silymarinum or its derivative, ligustrazine or its derivative, and ferulic acid or its derivative, and the medicinal auxiliary. Its advantage is low toxic by-effect to kidney.
US20120178729 Crystalline form i rosuvastatin zinc salt The present invention relates to crystalline Form I rosuvastatin zinc (2:1) salt, method of preparation thereof and use thereof as pharmaceutically active ingredient for the treatment of diseases related to lipid metabolism including hyperlipoproteinemia, hypercholesteremia, dyslipidemia and atherosclerosis.
US20120207773 Materials and methods for the development of an antigen-specific immune non-responsiveness state The present invention provides materials and methods for making a subject non-responsive to an antigen. Methods of the invention may comprise contacting the subject with the antigen and a compound that induces anergy. In some embodiments, the antigen may be an autoimmune antigen, examples of which include, but are not limited to acetylcholine receptor for myasthenia gravis, glutamic acid decarboxylase for type I diabetes mellitus and rheumatoid factor in rheumatoid arthritis, hi some embodiments, the present invention provides a method of transplanting an organ, tissue, or cells into a subject (e.g., a mammal such as a human).
WO2009082268A3 LIGANDS OF α-ADRENOCEPTORS AND OF DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THE USE THEREOF The invention relates to novel ligands, the broad spectrum of which simultaneously comprises alpha-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and seratinin receptors, including 5-HT7 seratinin receptors, as compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers and also in the form of pharmaceutically acceptable salts and/or hydrates, wherein: R1 is an aminogroup substituent, optionally substituted C1-C2 alkyl, acyl, heterocyclyl, alkoxycarbonyl and substituted sulphonyl; R2 is a cyclic group substituent, including a hydrogen atom, a halogen atom, optionally substituted C1-C4 alkyl, CF3, CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulphonyl; Ar is optionally substituted aryl, possibly annelated with heterocyclyl, or optionally substituted heterocyclyl; W is an optionally substituted CH2-CH=CH group, an optionally substituted C≡C group, an SO2 group; n=1 or 2; m=1, 2 or 3; a continuous line together with a dotted line following it (---) represent a single or a double bonds. Medicinal substances, pharmaceutical compositions containing the novel ligands in the form of medicinal substances, novel medicinal agents which are used for treating diseases and states of the central nervous system of human beings and animals, are also disclosed.
CA2850137A1 Protein kinase inhibitors (variants), use thereof in treating oncological diseases and a pharmaceutical composition based thereon The present invention relates to the treatment of oncological, chronic inflammatory and similar diseases with the aid of new families of chemical compounds having improved efficiency with regard to the inhibition of ?b1 kinase and mutant forms thereof, as well as other therapeutically significant kinases. It describes protein kinase inhibitors in the form of compounds of general formula (I) and compounds of general formula (II), or a tautomer, an individual isomer, a mixture of isomers, a pharmaceutically acceptable salt, a solvate or a hydrate thereof.
US20100330039 Schizochytrium Fatty Acid Synthase (FAS) and Products and Methods Related Thereto Disclosed are a fatty acid synthase (FAS) from Schizochytrium, biologically active fragments and homologues thereof, a nucleic acid sequence encoding such FAS, fragments and homologues thereof, the gene encoding Schizochytrium FAS, host cells and organisms that recombinantly express the FAS, host cells and organisms in which the expression and/or activity of the endogenous FAS has been attenuated, and various methods for making and using any of these proteins, nucleic acid molecules, genes, host cells or organisms.
US20110144037 Substrates and Inhibitors of Antiplasmin Cleaving Enzyme and Fibroblast Activation Protein and Methods of Use The presently disclosed and claimed inventive concepts include inhibitors of antiplasmin cleaving enzyme (APCE) and fibroblast activation protein alpha (FAP) which can be used in various therapies related to disorders of fibrin and α2-antiplasmin and abnormal cell proliferation. The presently disclosed and claimed inventive concepts also include substrates of APCE and FAP, which may be used, for example, in screening methods for identifying such inhibitors. The presently disclosed and claimed inventive concepts further include, but are not limited to, methods of treating or inhibiting atherosclerosis and thrombus disorders by altering the ratios of types of plasma α2-antiplasmin and to methods of treating conditions involving abnormal cell proliferation such as cancers.
WO2006084793A3 Film-coated tablets containing ibuprofen lysinate The invention relates to film-coated tablets containing ibuprofen lysinate with improved stability, bio-availability and increased acceptance (compliance) by patients and to the use of said film-coated tablets for producing a medicament for treating acute and/or chronic pain.
WO2013001449A1 Pharmaceutical compositions containing hydroxypropyl methylcellulose and/or hyaluronic acid and their use The present invention relates to pharmaceutical compositions containing hydroxypropyl methylcellulose and/or hyaluronic acid and optionally amino acids (glycine, proline, leucine, lysine and salts thereof) and their use in the prevention and/or treatment of gastroesophageal reflux disease.
CN101264058B Huperzine A and its derivative or salts sustained-release nanometer granule and preparing method thereof The invention provides huperzine A and slow releasing nanoparticles of ramification or arsoniumsalt of huperzine A, which comprises huperzine A, ramification or arsoniumsalt of huperzine A, and a carrier, wherein, the carrier comprises one or a plurality of components of the mixture of polylactic acid, glycolide-lactide copolymer, gelatin, chitosan, copolymer of polyethylene glycol and polylacticacid, copolymer of polyethylene glycol and glycolide-lactide, soybean phospholipids, soybean lecithin, lecithin and glycerol stearate. The slow releasing nanoparticles of ramification or arsoniumsaltof huperzine A is used for curing Alzheimer's disease, vascular dementia and other elderly diseases. The slow releasing nanoparticles can prolong the drug acting time, decrease the administration frequency, improve the bioavailability of huperzine A and ramification or arsoniumsalt of huperzine A, reduce the toxic and side effect of the drug, and improve the patient compliance for the drug.
US20080299218 Deuterium-enriched valsartan The present application describes deuterium-enriched valsartan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
CN102048701A Pitavastatin calcium enteric sustained-release micropill preparation and preparation method thereof The invention provides a pitavastatin calcium enteric sustained-release micropill preparation and a preparation method thereof, which can solve the problems that: (1) pitavastatin calcium is easily subjected to inversion of configuration under the condition that gastric juice has a low pH value, and has low stability, and (2) common tablets are released too quickly, so that active ingredients cannot fully achieve the effect of reducing cholesterol in the prior art. The technical scheme is that: the pitavastatin calcium enteric sustained-release micropill preparation comprises a medicine-containing pill core, an isolation layer, a sustained-release layer and an enteric layer from inside to outside, wherein the medicine-containing pill core comprises pitavastatin calcium and pharmaceutical excipients. The invention also provides a preparation method for the micropill preparation. The prepared micropill is not released in the gastric juice, and medicines are prevented from being exposed in the acid environment; by adopting microporous film coating technology, the medicines can be slowly released from the pill core, the blood concentration is kept balanced, the medicine taking frequency is reduced and the compliance of the patient is improved.
EP2465857A1 Methods for synthesizing heterocyclic compounds A method for synthesizing a heterocyclic compound includes: reacting 1-methylpiperazine with 5-chloro-2-nitroaniline at an internal temperature sufficient to provide a compound of Formula VIH The 1-methylpiperazine and the 5-chloro-2-nitroaniline are reacted in a solvent that comprises water in an amount greater than 50 percent by volume based on the amount of the solvent and/or are reacted in a solvent that comprises an organic solvent component that has a boiling point of greater than 100°C at atmospheric pressure.
WO2013047567A1 Corneal epithelial cell death inhibitor containing flavin adenine dinucleotide or salt thereof as active ingredient Flavin adenine dinucleotide or a salt thereof significantly curbs the decline in viable cell count of corneal epithelial cells induced by ultraviolet radiation, and thus can act as an inhibitor of corneal epithelial cell death induced by ultraviolet radiation.
CN101502561B Chinese patent medicine for treating bile reflux gastritis as well as gallbladder disease The invention relates to a Chinese patent medicine for treating bile reflux gastritis and gallbladder diseases. The raw materials for producing the Chinese patent medicine comprise 500-1000 parts of mirabilite or weathered substances thereof and 300-1000 parts of lightyellow sophora root. The Chinese patent medicine takes the mirabilite as a main drug, thereby being capable of clearing heat, detumescence, eliminating inflammation, removing stones, inducing urination, improving stool discharge, rapidly easing discomforts of gallbladder and bile duct, the lightyellow sophora root is taken as anadjuvant, thereby being capable of treating jaundice and anuria, having better effect of clearing heat and eliminating inflammation for liver and gall, inducing diuresis, freeing strangury and strengthening the excretion of internal heat of the liver and the gall, and the combination of the two can radically cure acute and chronic cholecystitis, cholangitis, gallbladder stones, bile duct stones and bile reflux gastritis.
US20090060888 Regulated transcription of targeted genes and other biological events Dimerization and oligomerization of proteins are general biological control mechanisms that contribute to the activation of cell membrane receptors, transcription factors, vesicle fusion proteins, and other classes of intra- and extracellular proteins. We have developed a general procedure for the regulated (inducible) dimerization or oligomerization of intracellular proteins. In principle, any two target proteins can be induced to associate by treating the cells or organisms that harbor them with cell permeable, synthetic ligands. To illustrate the practice of this invention, we have induced: (1) the intracellular aggregation of the cytoplasmic tail of the ζ chain of the T cell receptor (TCR)-CD3 complex thereby leading to signaling and transcription of a reporter gene, (2) the homodimerization of the cytoplasmic tail of the Fas receptor thereby leading to cell-specific apoptosis (programmed cell death) and (3) the heterodimerization of a DNA-binding domain (Gal4) and a transcription-activation domain (VP16) thereby leading to direct transcription of a reporter gene. Regulated intracellular protein association with our cell permeable, synthetic ligands offers new capabilities in biological research and medicine, in particular, in gene therapy.
EP2350051A1 Pyridine, bicyclic pyridine and related analogs as sirtuin modulators The present invention provides novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders relating to aging or stress, diabetes, obesity, neurodegenerative disease, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorder that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. The compounds are of general formula (III) wherein R1, R2, R", X, Y, W, Z1 and Z2 are as defined in the specification.
WO2006046402A1 Triglyceride metabolism controlling agent and containing the same, food, drink, food additive and pharmaceutical [PROBLEMS] To provide a triglyceride metabolism controlling agent that is derived from natural products, exhibiting a metabolism controlling potency to triglycerides and is extremely low in the possibility of side effects. [MEANS FOR SOLVING PROBLEMS] There is provided a triglyceride metabolism controlling agent comprising an apple extract or a hop bract extract as an active ingredient.
US7227022 Use of 2-amino-thiazoline derivatives as inhibitors of inducible no-synthase The present invention relates to a process for preparing 2-amino-thiazoline derivatives of formula (II): in which either Y is a methylene (CH2) and X is chosen from the following groups: O, NH, (C1–C4) N-Alkyl, N-Bn, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 or CHPh; or Y is a carbonyl (C═O) and X is chosen from the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl or N-5-pyrimidyl.
CN102219811A CA-4 derivatives and preparation method and medicinal application thereof The invention relates to the field of pharmaceutical chemistry, in particular to CA-4 derivatives (I) and a preparation method thereof, and the inhibitory effect of the CA-4 derivatives on tumor blood vessels. Pharmacological experiments prove that the compounds can be used for treating angiogenesis-related diseases such as various cancers and chronic inflammation, and other angiogenic diseases.
US20120141581 Capsule and powder formulations containing lanthanum compounds The present invention includes an oral pharmaceutical capsule comprising a shell, lanthanum carbonate or lanthanum carbonate hydrate, and a lubricant such as talc, wherein the shell encapsulates the lanthanum carbonate or its hydrate and the lubricant. Capsule shells comprise, for example, gelatin. The present invention also includes an oral pharmaceutical powder comprising lanthanum carbonate or lanthanum carbonate hydrate and a pharmaceutically acceptable excipient. The oral pharmaceutical capsules and powders of the present invention can be administered to treat a patient at risk of or suffering from hyperphosphatemia, at risk of or suffering from chronic kidney disease (CKD), at risk of or suffering from soft tissue calcification associated with CKD, or at risk of or suffering from secondary hyperparathyroidism.
WO2010118852A1 ( pyrazol-3-yl) -1, 3, 4-thiadiazol-2-amine and ( pyrazol-3-yl) -1, 3, 4-thiazol-2-amine compounds wherein: either X is N and Y is CR5 or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and Me; R2 is selected from H, OH, OMe and Me; each R3 is independently selected from C1-3alkyl, F, Cl, Br, CF3 and NH2; R4 is selected from Me, CF3, NO2 and CHF2; R5 is selected from H, Me and CHF2; R6 is selected from H and Me; and p is 0-3, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
US7067522 anticarcinogenic, antitumor, antiproliferative agents; focal adhesion kinase (FAK) and cyclin-dependent kinase (CDK) enzyme inhibitors Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.
US7338965 Enzyme inhibitors of beta-secretase which cleaves amyloid precursor protein present in Alzheimer's disease; Trisomy 21 (Down's Syndrome); Hereditary Cerebral Hemorrhage; cognition activators; Parkinson's disease The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. One embodiment of the invention relates to compounds having the structure: where Z is CR or N, and R1, R2 and R3 are as described in the specification.
US20110245256 Use of a pkc inhibitor The present invention demonstrates that chronic active BCR signaling through CD79A/B confers a strong dependence on downstream PKCb kinase signaling. Hence, provided herein is a method for inhibiting the growth of B-cell lymphoma having chronic active B-cell-receptor signaling, or inhibiting the growth of cancers with molecular lesions that lead to chronic active BCR signaling, by administering to a patient in need of such treatment a therapeutically effective amount of a PKC inhibitor or a use of a PKC inhibitor to inhibit the growth of B-cell lymphoma having chronic active B-cell-receptor signaling or to inhibit the growth of cancers with molecular lesions that lead to chronic active BCR signaling.
US20100279962 Monosebacate of pyrazole derivative The present invention provides a novel form of 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since bis[3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide] monosebacate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.
EP0870049B1 Complementary adenoviral vector systems and cell lines The present invention provides multiply replication deficient adenoviral vectors having a spacer in at least one replication deficient adenoviral region, as well as complementing cell lines therefor. Also provided are means of constructing the multiply replication deficient adenoviral vectors and methods of use thereof, e.g., in gene therapy.
WO2010025630A1 Sodium cholate-included prednisone intercalated layered double hydroxides and preparation method thereof The formula of the sodium cholate-included prednisone intercalated layered double hydroxides is provided, (M2+)1-x(M3+)x(OH-)2(C21H26O5)a(C24H39O5 -)x·mH2O, wherein x is 0.25-0.33 and a is 0.02-0.03. The preparation method for the sodium cholate-included prednisone intercalated layered double hydroxides comprises preparing sodium cholate micelle water solution, adding prednisone/chloroform solution in nitrogen ambient, stirring to volatilize chloroform to obtain sodium cholate-included prednisone solution, preparing mixed solution of magnesium nitrate and aluminum nitrate with Mg/Al molar ratio 2-3, dropping into the sodium cholate-included prednisone solution in nitrogen ambient, stirring, adjusting pH to 7-9, crystallizing at 70 centigrade degree for 65-75 hours, centrifugating with CO2-removing water 3-4 times, and drying at 60-70 centigrade degree for 12-24 hours. The drug delivery system of the sodium cholate-included prednisone intercalated layered double hydroxides has advantages of good thermal stability and sustained release effect.
CN102327220A Solid loratadine lipidosome preparation The invention provides a solid loratadine lipidosome preparation, which is mainly prepared from the following components according to weight part: 2.5 parts of loratadine, 50-100 parts of sphingomyelin, 2.5-25 parts of cholesterol, 0.5-2 parts of span 80, 1-2.5 parts of tween 80 and 85-295 parts of other general pharmaceutical excipients. The solid lipidosome preparation provided by the invention has the advantages of high entrapment rate, uniformity in grain size and long reservation time of a medicament in blood circulation; and the quality of a preparation product is improved and toxic or side effects are reduced. In addition, equipment used by a preparation method is simple, easy for operation and suitable for industrial large-scale production.
WO2010126435A1 Novel galactoside inhibitors of galectins The present invention relates to novel compounds having an effect as i.a. galectin inhibitors, to the use of said compounds as a medicament as well as for the manufacture of a medicament for treatment of disorders relating to the binding of galectin to receptors in a mammal, where in said galectin is preferably a galectin-3. The novel compounds are defined by the general formula: (I)
US7033578 Antimycotic nail varnish composition The present invention relates to a composition comprising a) at least one antimycotic agent and b) at least one film forming agent wherein component b) is a derivative of chitosan selected from hydroxyalkylchitosans and carboxyalkylchitosans and its use as a nail varnish. The present invention is further directed to the use of a water soluble film forming agent selected from hydroxyalkylchitosans and carboxyalkylchitosans as an additive in a nail varnish.
CN102391353A Walsuralactam A and preparation method and application to medicament thereof The invention provides novel Walsuralactam A (a compound in the formula I) with medical value and a method for extracting the compound from Walsura yunnanensis plants. Meanwhile, the invention also provides a medicinal composition and application of the compound and the medicinal composition thereof to preparation of a medicament for treating and preventing tumour, wherein the medicinal composition comprises the compound in the formula I, which is used as an active ingredient, and is used for treating and preventing the tumour.
WO2014025989A1 Compositions and methods for treating mood disorders or skin disease or damage Methods for the treatment of mood disorders and/or skin disease or damage (eczema, atopic dermatitis, or wrinkles, for example) can comprise administering an extracted prenylflavonoid to a subject experience the mood disorder or the skin disease or damage.
US20080221097 N-(3-Bromophenyl)-1-methyl-7-(1-piperidinylcarbonyl)-1H-imidazo[4,5-c]pyridin-4-amine hydrochloride salt; immune disorder, an inflammatory disorder, pain, rheumatoid arthritis, multiple sclerosis, osteoarthritis or osteoporosis The present invention relates to novel imidazopyridine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
CN102861021A Dry powder spray for rhinitis The invention, relating to the new treatment field of rhinitis sufferers, mainly discloses a dry powder spray for rhinitis prepared by fusing amoxicillin and vitamin B2 into ultrafine dry powder, wherein the ratio of amoxicillin to vitamin B2 is 10:1. The spray disclosed herein has the advantages of convenient usage, cost saving, no side effect, and quick effectiveness.
US7053230 Administering a combination of an omega-3 fatty acid and aspirin, to a patient suffering from inflammation, arthritis or cardiovascular diseases Aspirin triggered lipid mediators (ATLMs) are disclosed which are useful for the treatment of prevention of inflammation associated with various diseases, including ischemia.
CN1586465A Pain eliminating aerosol and its preparing method The present invention provides a kind of medicine pain eliminating aerosol packed in pressure container with special valve system and capable of being applied to skin surface or body cavity to produce local anesthesia or general anesthesia. Its production process includes dissolving material, mixing, sterilizing, packing, leakage test and other steps. The present invention has simple recipe, simple preparation process and convenient application, and may be used in treating burns, scalds and trauma with obvious curative effect.
US7754772 (2R)-2,3-bis(nitrooxy)propyl(2S)-2(6-methoxy(2-naphthyl)propanoate, used for treating inflammation, pain and fever; gastrointestinal disorders; wound healing agents; preventing gastrointestinal, renal and/or respiratory toxicities; side effect reduction The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
CN101112362A Dispersion tablets for treating and preventing upper respiratory tract infection The present invention discloses a drug compound which has good taste, contains acetaminophen, chlorpheniramine maleate, cloperastini hydrochloride, pseudoephedrine hydrochloride, caffeine and bromelain and can be dispersed uniformly and is used for curing the upper respiratory tract Infection; the invention further contains fillers, disintegrating agents, flow agents, lubricants, sweeteners and other pharmaceutical excipients, and the single dose thereof is the dispersible tablet form.
WO2009012425A3 Compositions including leukotriene antagonists and nsaids and methods of using the same Pharmaceutical compositions containing non-steroidal anti-inflammatory drugs (NSAIDs) and modified NSAIDs and leukotriene antagonists and methods for using such pharmaceutical compositions are provided herein. In a preffered embodiment naproxene 2- (methanesulfonyl) -ethyl ester is used in combination with Zileuton.
CN101314046B Cyclodextrin inclusion method for hair orchid native The invention provides a cyclodextrin inclusion method for erianin, which comprises the following steps that: (1) hydroxypropyl-beta-cyclodextrin is added into water and is stirred to be completely dissolved, the mass ratio of the hydroxypropyl-beta-cyclodextrin to the water is 1 to between 3 and 5; crystalline powder of the erianin is added with absolute ethyl alcohol and is completely dissolvedby ultrasonic vibration, and the mass ratio of the erianin to the absolute ethyl alcohol is 1 to between 500 and 2,000; (2) a hydroxypropyl-beta-cyclodextrin water solution is placed in a water bath and is stirred, then an erianin alcohol solution is dripped into the hydroxypropyl-beta-cyclodextrin water solution, and the adding amount is controlled that the mass ratio of the erianin to cyclodextrin is equal to between 1 to 8 and 1 to 11; the mixture continues to be stirred for 2 hours after the dripping is finished, is kept stand for 2 hours and then continues to be stirred for 1 hour; and (3) the mixed solution is placed in the water bath at a temperature of 55 DEG C to reclaim alcohol through pressure reduction concentration, and is placed in the water bath at a temperature of 75 DEG Cfor further concentration when the solution is translucent and glutinous, and a concentrated solution is dried under vacuum to produce a powder product.
WO2011052923A3 Novel 1,6-disubstituted indole compounds as protein kinase inhibitors Disclosed are a 1,6-substituted indole compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of cancers caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel indole compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.
US20080227815 Crystal of Indole Derivative Having Piperidine Ring and Process for Production Thereof A crystal of 1-[1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)-ethyl]piperidin-4-yl]-N-methyl-1H-indole-6-carboxamide fumarate which has peaks at chemical shifts of about 124.0 ppm and about 26.8 ppm in a 13C solid NMR spectrum.
WO2014131851A1 SALTS OF 2-AMINO-1-HYDROXYETHYL-8-HYDROXYQUINOLIN-2(1H)-ONE DERIVATIVES HAVING BOTH β2 ADRENERGIC RECEPTOR AGONIST AND M3 MUSCARINIC RECEPTOR ANTAGONIST ACTIVITIES The present invention is directed to crystalline addition salts of (i) 8-hydroxyquinolin-2(1H)-one derivatives and (ii) a hydroxycarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvates thereof.
EP2125736B1 Substituted acetophenones useful as pde4 inhibitors The present invention relates to a compound according to formula: (I); wherein X1, X2, X3, X4 and X5 independently of each other represent -CH- or N; or X3, X4 and X5 independently of each other represent -CH- or N, and Xi and X2 independently of each other represent C and form part of an additional 6- membered aromatic ring; R1 represents hydrogen, alkyl, alke nyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, -CH2-C(O)NR-R', alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, alkylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent -CH- or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hyd rates, or solvates thereof. The invention relates further to processes for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
CN202568934U Tablet capsule filled with glipizide solid preparations and metformin solid preparations The utility model relates to an oral hard capsule, in particular to a tablet capsule filled with metformin tablets and glipizide tablets. The tablet capsule is composed of a capsule body and the tablets in the capsule body, the capsule body comprises an upper capsule body and a lower capsule body, and at least one tablet with active ingredients of metformin and at least one tablet with active ingredients of glipizide are filled in the capsule body. The tablet capsule filled with the metformin tablets and the glipizide tablets is better in stability and convenient to process as the active ingredients in the capsule do not contact with one other.
CN103356723A Cooling paste for children and preparation method thereof The invention relates to a cooling paste for children and a preparation method thereof, and solves treatment and medication problems for children having a fever. The technical scheme is that the cooling paste is prepared from raw materials, by weight, comprising 10-14% of sodium polyacrylate, 2.2-6.2% of edible gelatin, 2-8% of sodium carboxymethylcellulose, 0.4-1% of citric acid, 4-26% of carbomer, 2-6% of astragalus polysaccharides, 10-20% of a distillate of the root of Chinese thorowax, 8-11% of kaolin or diatomite, 20-40% of glycerin, 6-12% of propylene glycol, 0.2-6.6% of menthol and 0.04-0.24% of disodium dihydrogen ethylenediaminetetraacetate. The cooling paste has advantages of scientific and reasonable components, abundant raw materials, easy production, usage convenience and good effects. The cooling paste can be effectively used for treating the children having a fever, and is an innovation in medicines used for treating the children having a fever.
EP2632459A2 Method of treating neuroendocrine tumors Methods and compositions for treating neuroendocrine tumors are disclosed.
CN1939295A Baical skullcap root dropping balls and making method thereof A dripping pill of scutellarin for treating anaphylactic dermatitis is prepared from scutellaside (20-30 Wt%) and polyethanediol 4000 (65-80). Its preparing process is also disclosed.
WO2010011347A3 Clip inhibitors and methods of modulating immune function The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmune disease, allergic disease transplant and cell graft rejection, cancer, bacterial infection, HIV infection, and AIDS.
WO2007047405A1 Ddc compositions A composition comprising from 1 % to 3% dDC which is aqueous and ophthalmically acceptable is disclosed herein.
EP0944604B1 Guanidinyl heterocycle compounds useful as alpha-2 adrenoceptor agonists This invention involves compounds having structure (I) as described in the Claims; and enantiomers, optical isomers, stereoisomers, diastereomers, tautomers, addition salts, biohydrolyzables amides and esters thereof, as well as pharmaceutical compositions comprising such novel compounds. The invention also relates to the use of such compounds for preventing or treating disorders modulated by alpha-2 adrenoceptors.
CN103505407A Multi-chamber bag packaged moxifloxacin hydrochloride/glucose aqueous solution preparation The invention discloses a multi-chamber bag packaged moxifloxacin hydrochloride/glucose aqueous solution preparation which comprises at least two chamber bags, chambers are separated by weak sealing parts, wherein moxifloxacin hydrochloride and glucose are respectively stored in different chambers, a chamber storing the glucose and a chamber storing the moxifloxacin hydrochloride are adjacent, the moxifloxacin hydrochloride is stored in the chamber in a form of an aqueous solution or powder, and the glucose is stored in the form of an aqueous solution. Through extrusion of the chambers filled with solutions, the weak sealing parts are opened, the chambers are connected to form a closed system to mix to obtain the clinically used moxifloxacin hydrochloride/glucose injection, after mixing, the concentration of the moxifloxacin hydrochloride is 0.16%-0.4%, and the concentration of the glucose is 5%. The multi-chamber bag packaged moxifloxacin hydrochloride/glucose aqueous solution preparation solves the problems that at high temperature, moxifloxacin has no long term compatibility with the glucose, insoluble particles may be produced, particle solubility may be reduced by sodium chloride and the insoluble particles may also be produced due to low temperature.
US6908943 Use of γ-tocopherol and its oxidative metabolite LLU-α in the treatment of disease The present invention is generally related to the discovery of the therapeutic benefit of administering γ-tocopherol and γ-tocopherol derivatives. More specifically, the use of γ-tocopherol and racemic LLU-α, (S)-LLU-α, or γ-tocopherol derivatives as antioxidants and nitrogen oxide scavengers which treat and prevent high blood pressure, thromboembolic disease, cardiovascular disease, cancer, natriuretic disease, the formation of neuropathological lesions, and a reduced immune system response are disclosed.
CN102204903A Application of peperomin E and peperomin B compounds to medicament for suppressing angiogenesis The invention relates to application of peperomin E and peperomin B compounds to a medicament for suppressing angiogenesis. The invention has the advantages that: the invention provides novel application of peperomin E and peperomin B; and as proved by experiments, the peperomin E and the peperomin B have anti-angiogenesis activities and can be taken as angiogenesis suppressants. In the invention, the anti-angiogenesis functions of the peperomin E and the peperomin B are found for the first time. The peperomin E and the peperomin B can be taken as angiogenesis suppressants for application to the treatment of tumor, arthritis, skin and eye diseases, new vessel dependent and new vessel relevant diseases such as atherosclerosis and the like.
CN102885778A Active carbon paclitaxel nano-drug delivery system, and preparation method and application thereof The invention relates to a nano active carbon drug delivery system of paclitaxel drugs and also relates to a preparation method of the nano active carbon drug delivery system of the paclitaxel drugs and an application of the nano active carbon drug delivery system of the paclitaxel drugs in preparing drugs for preventing and/or treating paclitaxel adaptation diseases such as ovarian cancer, breast cancer, lung cancer, colorectal cancer, melanoma, head and neck cancers, lymphoma and cerebroma. The active carbon paclitaxel nano-drug delivery system has a function target to lymphoid tissues and tumor tissues and can deliver paclitaxel drugs to tumor tissues in a targeted manner, so that the curative effect of drugs is improved and the side effect of drugs is reduced.
US7763646 beta-secretase inhibitors such as N-(3,5-difluorobenzyl)-N-{(2R)-2-hydroxy-3-[(3-iodobenzyl)amino]propyl}-5-methyl-N',N'-dipropylisophthalamide, used for reducing amyloid beta peptide formation The invention relates to compounds of formula (I). Useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
CN102716149A Calcium carbonate-D3 effervescent tablet and preparation method thereof The invention discloses a calcium carbonate-D3 effervescent tablet and a preparation method thereof and belongs to the technical field of medicinal preparations. The calcium carbonate-D3 effervescent tablet comprises calcium carbonate, vitamin D3, one or more acid sources, one or more diluents, one or more lubricants, one or more binders, essence and a sweetener. The preparation method comprises the following steps of mixing calcium carbonate, the one or more acid sources, the one or more diluents, the one or more binders and vitamin D3, preparing the mixture into a soft material by absolute ethanol, carrying out granulation, drying and finishing, uniformly mixing the one or more lubricants, the essence, the sweetener and the particles obtained by the previous step, and carrying out tabletting and vacuum packaging. The calcium carbonate-D3 effervescent tablet has a high calcium absorption rate, solves the problem that the existing calcium carbonate-based calcium supplement product consumes an excess of gastric acid and causes dyspepsia, contains vitamin D3, promotes full absorption of calcium, satisfies the requirements of different groups of people, riches dosage forms of calcium products, has a good taste, and is convenient for taking and carrying.
CN101773480A Preparation method of Nnanocrystal preparation containing docetaxelDuoxitasai and method for preparing a freeze-drying agent thereof The invention discloses apreparation methods of nanocrystal preparation containing docetaxelDuoxitasai and a method for preparing a freeze-drying agent thereof. The methods comprises the following steps of: 1, dissolving a surfactant into an aqueous solution to form a solution A; 2, dispersing Duoxitasaidocetaxel in the solution A obtained in step 1 to form a suspension B; 3, shearing the suspension B at a high speed for 1-3 minutes to form a primary emulsion C; 4, carrying out adopting a high pressure emulsion homogenization method on the primary emulsion C to prepare formthe primary emulsion C into a nanocrystal preparation of docetaxelDuoxitasai; 5, adding 0.5-20% (in by mg/ml) of freeze drying protective agents to the nanocrystal preparation, filtering, and sterilizing; and 6, removing water content by freeze drying to prepare dried nanocrystal freeze-drying agent containing the docetaxelDuoxitasai. The nanocrystal freeze-drying agent containing the docetaxelDuoxitasai prepared by the preparation process has the advantages of high safety, good stability, low toxic or side effect, reliable curativeng effect, and the like.
EP1372649B1 Novel medicament compositions on the basis of anticholinergics and pde iv inhibitors The invention relates to novel medicament compositions on the basis of anticholinergics and PDE IV inhibitors, and to the use thereof in the therapy of respiratory tract diseases.
CA2850848A1 Composition for the treatment of fistula A composition for use in the treatment of fistula, the composition comprising activated carbon.
CN103599186A Compound lotus root starch preparation The invention discloses a compound lotus root starch preparation, which is mainly prepared from vitamin D, lotus root starch, walnut powder and casein phosphopeptides as main raw materials.
EP1923054A1 Fast disintegrating pharmaceutical composition comprising an S1P agonist or modulator The present invention provides a fast disintegrating solid pharmaceutical composition suitable for oral administration comprising a S1 P receptor agonist and/or modulator.
WO2005000402A3 Anti-adhesion composites and methods os use thereof Described herein are composites that inhibit or reduce adhesion between two or more tissues. Also described herein are methods of using the composites.
CN103142762A Anti-cancer pharmaceutical composition and application thereof The invention relates to an anti-cancer pharmaceutical composition and an application thereof. The composition consists of effective anti-cancer ingredients and a pharmaceutical adjuvant. The effective anti-cancer ingredients comprises (-)-epigallocatechin-3-0-gallate which is extracted from green tea and a phosphodiesterase inhibitor, wherein the mass ratio of the phosphodiesterase inhibitor to the (-)-epigallocatechin-3-0-gallate is (0-2):(1-6). The anti-cancer pharmaceutical composition has the advantages of high efficiency, low cost, easiness in obtaining materials and small toxic or side effect.
EP2668851A1 Liver function-improving agent The present invention provides a liver function-improving agent or an inhibitor of fat accumulation in the liver, which contains maltitol as an active ingredient. The present invention also provides a medicament for the prevention and/or treatment of hepatic dysfunction, which contains maltitol as an active ingredient.
US7618649 For therapy of nasal and non-nasal symptoms of perennial and seasonal allergic rhinitis A bilayer solid composition comprising (a) an immediate release first layer comprising an anti-allergic effective amount of desloratadine and at least one pharmaceutically acceptable excipient and (b) a sustained release second layer comprising an effective amount of a nasal decongestant, e.g. pseudoephedrine sulfate and a pharmaceutically acceptable sustained release agent wherein the composition contains less than about 2% of desloratadine decomposition products is disclosed. A solid composition comprising an anti-allergic effective amount of desloratadine and at least one, and preferably two pharmaceutically acceptable antioxidants is also disclosed.
EP1341758B1 Coniosetin and derivatives thereof, method for producing the same and use thereof The invention relates to novel active agents (coniosetin and coniosetin derivatives) of formula I, which are produced by the micro-organism Coniochaeta ellipsoidea Udagawa (DSM 13856) during fermentation, R, R2, R3, R4, R5, X, X2, X3 and X4 having the meanings given. The invention also relates to chemical derivatives of coniosetin, to a method for producing them and to the use of the same as medicaments.
WO2008024298A1 Bis(thiohydrazide amides) for inhibiting angiogenesis Disclosed herein- are methods of inhibiting angiogenesis in a subject in need thereof with bis(thio-hydrazide amides) represented by a formula selected from Structural Formulas (I)- (IX) or pharmaceutically acceptable salts thereof.
CN101285030A Brewing method of special vinegar for reducing blood sugar The invention provides a method for making special vinegar for reducing blood sugar. The method comprises the following steps of: (1) adopting pure honey without cane sugar added with 0.7 to 2g of xylo-oligosaccharide in per 100ml pure honey for evenly mixing; (2) selecting the patent product which is 99 Ages Vitamin Vinegar (patent number: ZL90102404.X) produced by Luoyang 99 Ages Health Food Factory for evenly mixing according to a proportion of adding 0.7 to 2g of the xylo-oligosaccharide in per 100ml pure honey; (3) completely mixing the mixture of step (1) and step (2) according to a proportion of 1 to 1, and adding 10 to 15 times of water at 50 DEG C to receive the special vinegar for reducing blood sugar. The special vinegar for reducing blood sugar has the characteristics of good effect of reducing the blood sugar, simple technology, easy popularization and so on.
US20120083510 Perfluorocarbons for use in treating pruritus The subject application provides a method of treating pruritus comprising administering to the skin of a subject afflicted with pruritus an amount of a perfluorocarbon effective to treat the pruritus. The subject application also provides a method of alleviating a symptom of psoriasis comprising administering to the skin of a subject afflicted with psoriasis an amount of a perfluorocarbon effective to alleviate the symptom of psoriasis. The subject application also provides a perfluorocarbon composition for use in treating a subject afflicted with pruritus or psoriasis. The subject application further provides a pharmaceutical composition comprising an amount of a perfluorocarbon for use in treating pruritus or psoriasis.
EP1069893B1 Use of dexmedetomidine for icu sedation The present invention relates to a method of sedating a patient while in the intensive care unit (ICU). The method comprises administering dexmedetomidine or a pharmaceutically acceptable salt thereof to a patient in need thereof for a sufficient time period. Further, the present invention relates to a method of sedating a patient in the ICU by administering dexmedetomidine or a pharmaceutically acceptable salt thereof, wherein dexmedetomidine is essentially the sole active agent or the sole active agent.
EP2556072A1 2-phenyl benzothiazole linked imidazole compounds as potential anticancer agents and process for the preparation thereof The present invention provides 2-phenyl benzothiazole linked imidazole compounds of formula A as anti cancer agent against fifty three human cancer cell lines. (General formula A) wherein (II) R=H or OCH3; R1=H, F or OCH3; R2=H or OCH3; R3=H, NH2, F or OCH3; R4=H, NH2 or OCH3; R5=H, NH2, F, CF3 or OCH3; R6=H or OCH3; R7=H or OCH3; R8=H or OCH3.
EP1278535B1 Uses of tgap7 for the modulation of leucocyte activation Described are pharmaceutical compositions comprising polynucleotides encoding TGAP7 protein or a biologically fragment thereof. Furthemore, pharmaceutical compositions are described which comprise vectors comprising the aforementioned polynucleotides and/or host cells transformed therewith. Additionally, pharmaceutical compositions comprising antisense constructs to be aforementioned polynucleotides are described. Furthermore, methods and uses for modulating immune responses through the TGAP7 protein as well as pharmaceutical compositions comprising agents which act on the TGAP7 protein are described. Also, the use of said polynucleotide, vector, protein or antibody for the preparation of diagnostic and pharmaceutical compositions for use, inter alia, in organ transplantation, for the treatment of autoimmune, allergic or infectious diseases, or for treatment of tumors is provided.
DE102004061002A1 New (5'S)-2',4'-dicyclopentyl -3'-9(S)-fluoro(4-(trifluoromethyl) phenyl)methyl)-5',8' -dihydro-6'H-spiro(cyclopropane-1,7'-quinoline)- 5'-ol is a cholesterol ester transfer protein inhibitor useful for treating e.g. coronary heart diseases (5'S)-2',4'-Dicyclopentyl-3'-{(S)-fluoro[4-(trifluoromethyl)phenyl]me thyl}-5',8'-dihydro-6'H-spiro[cyclopropane-1,7'-quinoline]-5'-ol (I) and its salts, solvates and solvates of the salts are new. (5'S)-2',4'-Dicyclopentyl-3'-{(S)-fluoro[4-(trifluoromethyl)phenyl]me thyl}-5',8'-dihydro-6'H-spiro[cyclopropane-1,7'-quinoline]-5'-ol of formula (I) and its salts, solvates and solvates of the salts are new. Independent claims are also included for: (a) the preparation of (I); and (b) a medicament comprising (I) in combination with an inert, non-toxic, pharmaceutically acceptable additives. [Image] - ACTIVITY : Cardiant; Vasotropic; Antilipemic; Antiarteriosclerotic; Anorectic; Cerebroprotective; Neuroprotective; Nootropic. - MECHANISM OF ACTION : Cholesterol ester transfer protein (CETP) inhibitor. The ability of (I) to inhibit cholesterol ester transfer protein was tested using CETP-fluorescence test in human plasma. The results showed that the median inhibitory concentration of (I) was 80 nM.
WO2006096577A3 Methods of preventing and treating opioid bowel dysfunction Methods of preventing and treating opioid bowel dysfunction are disclosed. In addition, methods of increasing the frequency of spontaneous complete bowel movements, methods for improving the quality of life of a patient suffering from opioid bowel dysfunction, methods for reducing a patient's dependence on laxatives, and methods for preventing or treating pain are also disclosed.
US7183273 Administering compounds such as N-(2-pyridinylmethyl)-N'-(6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl)-1,4-benzenedimethanamine for therapy of disease mediated by a chemokine receptor Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.
US7417064 3-aryloxy/thio-3-substituted propanamines and their use in inhibiting serotonin and norepinephrine reuptake There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; with the proviso that, when Z is H, then Y may not be optionally substituted phenyl or optionally substituted naphthyl.
CN1837213A Bilobalide A derivatives and pharmaceutical application thereof The invention provides a bilobalide A derivative and the use in pharmacy, wherein the bilobalide A derivative has a structural formula disclosed in the specification, R1 represents -X-Ar, -X-Z-Ar, -X-COOH, -CO-Ar, -SO2-Ar, -X-Het, X1-CO-X2-NR4R5 or -X-NR4R5, wherein X, X1, X2 represent C1-C8 alkylidene, Z represents C, O, S or N, Ar represents phenyl, pyridinyl, naphthyl, pyrimidinyl, or quinoline.
WO2007000998A1 BIS(ARYLMETHYLIDENE)ACETONE COMPOUND, ANTI-CANCER AGENT, CARCINOGENESIS-PREVENTIVE AGENT, INHIBITOR OF EXPRESSION OF Ki-Ras, ErbB2, c-Myc AND CYCLINE D1, β-CATENIN-DEGRADING AGENT, AND p53 EXPRESSION ENHANCER It has been demanded to improve the poor solubility of curcumin to develop an anti-tumor compound capable of inhibiting the proliferation of various cancer cells at a low concentration. Thus, disclosed is a novel synthetic compound, a bis(arylmethylidene)acetone, which has both of an excellent anti-tumor activity and a carcinogenesis-preventive activity. A bis(arylmethylidene)acetone (i.e., a derivative having a curcumin skeleton) which is an anti-tumor compound and has a carcinogenesis-preventive activity is synthesized and screened. A derivative having enhanced anti-tumor activity and carcinogenesis-preventive activity can be synthesized.
CN102657658A Medicine composition for treating myocardial infarction, vascular circulatory disturbance and thrombosis The invention belongs to the technical field of medicines and particularly relates to a medicine composition for treating diseases such as myocardial infarction, vascular circulatory disturbance and thrombosis. The medicine composition contains alprostadil. The medicine composition comprises the alprostadil with the weight percentage larger than or equal to 90% and smaller than 100% and prostaglandin H2 with the weight percentage larger than 0 and smaller than or equal to 10%. The medicine composition is determined through pharmacology experiments and toxicology experiments.
CN102796157A Caudatin derivative and medicinal composition and application thereof The invention discloses a caudatin derivative of a general formula (I). R1, R2, R3 and R4 are respectively one or combination of aromatic acyl, substituted aromatic acyl, heteroaromatic acyl, substituted heteroaromatic acyl, dicarboxylic monoacyl HOOC-M-CO- and inorganic acid group; and M in the HOOC-M-CO- is alkylene, aryl, substituted aryl, heterocyclic radical, substituted heterocyclic radical or alkylene. The invention also discloses a medicinal composition using the caudatin derivative as an active ingredient, a preparation method for the caudatin derivative and application of the derivative and the medicinal composition thereof in anti-hepatitis B inhibitor medicaments and anti-hepatitis B medicaments.
EP1761492B1 1-benzyl-4-¬(5,6-dimethoxy-1-indanone)-2-yl methyl piperidine oxalate (donepezil oxalate) and its polymorphs The present invention discloses a novel oxalate salt of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl] 5 methyl piperidine commonly known as Donepezil (I), its polymorphic forms and method of preparation thereof.
CN101307049A Alkaloid compounds, method for preparing same and applications as enzyme inhibitors The invention relates to an alkaloid compound, a method for preparing the alkaloid compound and an application of the alkaloid compound as enzyme inhibitor. During preparation, strain culture is first carried out to a marine fungus in a culture medium, and then fermentation culture is carried out to the fungus in a fermentation culture medium; obtained fermentation liquid is filtered to eliminate mycelium; filtrate is heated, concentrated and extracted through ethyl acetate; chromatographic separation is carried out, and after obtained eluent is concentrated, penicillazine is obtained; bromine or manganese dioxide is added to a solution dissolving the Penicillazine, and then Penicillazines 1 and 2 are respectively obtained after reaction; or acetic anhydride is added to a solution dissolving the Penicillazine 2, and then Penicillazines 3 and 4 are obtained after reaction. An alkaloid derivative derived from the marine fungus can effectively inhibit human topoisomerase I, can be used for developing enzyme inhibitor medicine, and has raw materials that can be produced in large scale.
US8048452 Pharmaceutical compositions of cholesteryl ester transfer protein inhibitor A pharmaceutical composition comprises a solid amorphous dispersion of a cholesteryl ester transfer protein inhibitor and a concentration-enhancing polymer.
US20100063030 Benzenesulfonyl Compounds and the Use Thereof The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
CN102302451A Honokiol submicroemulsion injection and production method thereof The invention relates to a honokiol submicroemulsion injection and a production method thereof, and can effectively solve the problems of production and clinical requirement of anti-tumor medicaments. According to the technical scheme of the invention, the injection comprises the following components in percentage by weight: 0.01 to 3.0 percent of honokiol, 0.1 to 30 percent of injection vegetable oil, 0.01 to 6.0 percent of emulsifier, 0.001 to 3 percent of auxiliary emulsifier, 0.001 to 0.3 percent of antioxidant, 0.001 to 10 percent of iso-osmotic adjusting agent, 0.000001 to 2 percent of pH regulating agent, and the balance of water. The honokiol submicroemulsion injection has the advantages of scientific composition, simpleness in preparation process, stable and controllable quality and low cost, and is suitable for industrial production; and the preparation provided by the invention has high drug loading rate and envelopment rate, can be stably stored for a long time, the medical effect of the honokiol better can be better exerted and the toxic and side effects of the honokiol better can be reduced, and thus the preparation is a great pharmaceutical innovation.
US20080090881 Treatment of diabetes with thiazolidinedione and metformin A method for the treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof, in a mammal which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitiser and a biguanide antihyperglycaemic agent, to a mammal in need thereof and a pharmaceutical composition comprising an insulin sensitiser and a biguanide antihyperglycaemic agent.
CN101883794A Novel chondroitin sulfate having decreased molecular weight and use thereof It is intended to provide a chondroitin sulfate having a decreased molecular weight which is useful as an inhibitor of peritoneal disorder caused by long-term use of a peritoneal dialysis fluid containing glucose or a polysaccharide of glucose as an osmotic substance or is useful as an osmotic substance in a peritoneal dialysis fluid. The chondroitin sulfate having a decreased molecular weight of the invention as a resolution means is characterized in that it has a weight average molecular weight of from 1000 to 20000 and comprises a constituent disaccharide unit represented by the following structural formula in an amount of from 65% to 100% (molar ratio) of the total. -[4GlcAbeta1-3GalNAc(6S)beta1]-] In the formula, GlcA represents a D-glucuronic acid residue; GalNAc represents a N-acetyl-D-galactosamine residue; beta1-3 represents a beta1-3 glycosidic linkage; beta1-4 represents a beta1-4 glycosidic linkage; and (6S) indicates that a group at the 6th position in the monosaccharide residue is sulfated.
WO2012105573A1 CYCLIC SULFONIUM SALT, PROCESS FOR PRODUCTION OF SAME, AND α-GLUCOSIDASE INHIBITOR COMPRISING SAME Provided is a novel cyclic sulfonium salt compound which is useful for the prevention or treatment of diabetes and the like. The present invention relates to a novel cyclic sulfonium salt compound represented by general formula (I) or (II), an isomer or solvate of the compound, or a pharmaceutically acceptable salt of the compound or the isomer or solvate. The present invention also relates to an α-glucosidase inhibitor, a pharmaceutical composition for preventing or treating diabetes, and an anti-diabetes food, each of which comprises the compound represented by general formula (I) or (II) and the like.
EP2332540A1 Administration of ranolazine for the treatment of diabetes Methods comprising the administration of ranolazine are provided for treating diabetes, lowering plasma level of HbA1c, glucose plasma levels, total cholesterol plasma level, and/or triglyceride plasma level while increasing HDL cholesterol levels and delaying onset of diabetic retinopathy in a diabetic, pre-diabetic, or non-diabetic mammal while minimizing undesirable side effects.
CN1803793A Razole derivatives and application thereof The invention relates to the derivatives and the salts having a general formula (I) and (II), wherein R1 is low level alkyl or halogen atom substituted low level alkyl, R2 is C1-4 straight chain or branched chain alkyl, R3 represents hydrogen, Li, Na or K.
US20080146554 Substituted Cycloalkyl Derivatives, Process for the Manufacture thereof and Use thereof as Medicament The present invention relates to compounds of formula 1 wherein the groups R1, R2, R3, R4, R5, R6, R7, R8, n, m and X may have the meanings given in the claims and in the specification, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.
US20140271541 Sphingosine-1-phosphate receptor agonists in the treatment of demyelinating disorders Disclosed are pharmaceutical combinations comprising at least one S1P receptor agonist, as well as a method for treating demyelinating diseases, e.g. multiple sclerosis or disorders associated therewith or Guillain-Barré syndrome, comprising co-administration, e.g. concomitantly or in sequence, of a therapeutically effective amount of a) an S1P receptor agonist, and b) at least one co-agent shown to have clinical activity against at least one symptom of a demyelinating disease.
CN103211813A Pharmaceutical composition containing clotrimazole The invention relates to a pharmaceutical composition containing clotrimazole and particularly relates to a pharmaceutical composition. The pharmaceutical composition contains metronidazole, clotrimazole, chlorhexidine acetate, sodium carboxymethyl starch, sodium carboxymethylcellulose, glycerine and water. The pharmaceutical composition disclosed by the invention has favorable pharmaceutical properties.
CN101559193A Mongolian preparation for treating hyperplasia of mammary glands The invention discloses a Mongolian preparation for treating hyperplasia of mammary glands. The Mongolian preparation is prepared from the following raw materials: round cardamon seed, motherwort, lilac flower, cape jasmine, Gymnadenia conopsea, nutmeg, Chinese eaglewood, seabuckthorn fruit, Manchurian Tubergourd fruit, bark of tree falsespiraea, myrobalan fruit, galangal, safflower, costus root, artificial cow-bezoar, Chinese juniper, faeces of flying squirrel, acorn, elecampane root, hairy antler, junzhen, Chinese caterpillar fungus, borax, flavescent sophora root, toosendan fruit, madder root, flower of loquat, lac, lithosperm root and Chinese globeflower. The Mongolian preparation can be used for treating the hyperplasia of mammary glands and has the advantages of obvious curative effect, convenient administration, and no toxic and side effect.
CN101768081A Inhibitor of fatty acid synthase and application thereof The invention discloses an inhibitor of fatty acid synthase and application thereof, comprising the following active ingredients: 5 galloyl group gluconic acid, methyl gallate and quercetin-3-O-L-rhamnoside. The mass of three active ingredients in per gram of the inhibitor of fatty acid synthase are sequentially as follows: 18-20mug, 2-3mug, 1-2mug. The inhibitor of fatty acid synthase not only can be applied to preparation of weight loss drugs, preparation of anti-cancer drugs, but also can be widely applied to additives for foods, health products, as well as daily chemicals.
CN101053554A Ginkgolide B powder injection and its preparation method The invention discloses a Ginkgolide B powder injection, which is characterized in that: it is a powder injection consisting of main medcine and pharmacological acceptable filter aid, excipient and stabilizer. Said main medicine is Ginkgolide B, and filter aid is meglumine, and excipient is mannitol or dextran 40, and stabilizer is EDTA-2Na or EDTA-CaNa. The weight ratio is: Ginkgolide B:EDTA-2Na or EDTA-CaNa:mannitol or dextran 40 = 1:0.5-3:0.01-2:1-20. The preparation solves the problems such as Ginkgolide B indissolvable problem, redissolve clarity and stability.
WO2012149083A1 Ppar-sparing thiazolidinediones for the treatment of kidney related diseases The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing PKD.
CN102993193A Use of nitrogen-3-isoxazolyl-3-4-thienyl-pyrimidyl sulfonyl propanamide derivative in preparing anti-tumor medicines The invention belongs to the field of a medicine, in particular to the use of a nitrogen-(4,5-bihydroisoxazole-3-yl)-3-(4-(thiophene-2-yl)-pyrimidine-2-sulfonyl) propanamide derivative in preparing anti-tumor medicines. The invention solves the technical problem that a novel compound is provided for the medicine for inhibiting tumor metabolism. The technical scheme provided by the invention is to provide the use of a nitrogen-(4,5-bihydroisoxazole-3-yl)-3-(4-(thiophene-2-yl)-pyrimidine-2-sulfonyl) propanamide derivative in preparing anti-tumor medicines and the derivative is shown as formula I. According to the invention, the compound shown as formula I has a good anti-tumor effect creatively, and can be used to prepare an anti-tumor medicine composition. A novel selection for the field of preparing the anti-tumor medicines is provided, and the derivative has a good application prospect.
WO2010096677A3 Dihydrolipoic acid derivatives comprising nitric oxide and therapeutic uses thereof Compounds are provided that comprise dinitroso-derivatives of dihydrolipoic acid. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating various diseases and disorders, including angina, hypertension, diabetes, dyslipidemia, renal insufficiency, myocardial infarction, stroke, atherosclerosis, and the target organ damage that accompanies these various diseases and disorders, are further provided. The compounds are useful in improving vasodilation, reducing low-density lipoprotein oxidation, and reducing inflammation in a subject.
WO2013163279A1 Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
CN103463071A Application of Lycojaponicumin C in preparation of medicines for resisting lung cancer metastasis The invention discloses an application of Lycojaponicumin C in the preparation of medicines for resisting lung cancer metastasis, belonging to the technical field of new applications of medicines. The Lycojaponicumin C can be used for inhibiting the movement and metastasis capacity of tumor cells. The application of the Lycojaponicumin C in the preparation of the medicines for resisting lung cancer metastasis is disclosed for the first time. As the skeleton type of the Lycojaponicumin C belongs to a brand-new skeleton type, the Lycojaponicumin C has unexpected strong inhibitory activity on the metastasis of lung cancer cells.
WO2013012118A1 Novel phenylester compound and pharmaceutical compositions for preventing or treating inflammatory diseases comprising the same The present invention relates to a novel compound, named 2-ethoxy-4-(3-hydroxy-2-oxopropyl) phenyl 2-oxoacetate or a pharmaceutically acceptable salt thereof, which shows anti-inflammatory activity, and a method for preparing the same. Also, a pharmaceutical composition for preventing or treating inflammatory diseases, having the compound or a pharmaceutically acceptable salt thereof as an active ingredient is disclosed. Having therapeutic activity for inflammatory diseases, the phenylester compound is also applicable to a quasi-drug composition, a health functional food composition, and a cosmetic composition, all of which are intended to prevent or improve inflammation. Also, a method is provided for treating an inflammatory disease by administering the pharmaceutical composition to a subject in need thereof. As a natural materials, the novel phenylester compound can be used as a safe therapeutic relatively free of fungal infection or other side-effects, compared to synthetic medicines.
WO2008041460A1 Active oxygen scavenger, activating agent and collagen production promoter each comprising cacalol [PROBLEMS] To provide a active oxygen scavenger which has an excellent active oxygen scavenging activity, an activating agent or an anti-aging agent which has an excellent cell-activating activity and an excellent anti-aging activity, can stand long use satisfactorily and is safe, and a collagen production promoter which has a significant collagen production promoting activity, can stand long use satisfactorily, and is safe, and also provide a method for producing a plant extract having a high cacalol content by removing chlorophyll from a plant extract produced from a plant containing cacalol. [MEANS FOR SOLVING PROBLEMS] Disclosed are a active oxygen scavenger, an activating agent, an anti-aging agent and a collagen production promoter each comprising cacalol. Further disclosed is a method for producing a cacalol-containing plant extract, characterized by reducing the chlorophyll content of the cacalol-containing plant extract compared to that of the original extract by using a mixture composed of water and a hydrophilic organic solvent at a proper mixing ratio.
CN101953838A Application of rutaecarpine in treating psoriasis The invention relates to an application of 8, 13-Dihydro-indolo [2',3':3,4] pyrido [2,1-b] quinazolin-5 (7H)-one compound (rutaecarpine) in treating the psoriasis. When the psoriasis is treated by the substance, the substance is partially applied in the form of ointment, gelling agent, sticking stuff, lotion, liniment and film coating agent and the like. The structure formula of the rutaecarpine is as follows: C16H13N3O.
CN103417571A Composition for treating chicken mycoplasma respiratory infection and preparing method thereof The invention discloses a composition for treating chicken mycoplasma respiratory infection and a preparing method of the composition. The composition comprises, by weight, 1-10% of erythromycin thiocyanate, 40-90% of ammonium chloride and the balance anhydrous dextrose. According to the composition, the erythromycin thiocyanate is used as a main ingredient for resisting mycoplasmas, is effective in various mycoplasmas causing the chicken respiratory infection, is taken orally and can be absorbed, and can effectively treat mycoplasma infection of respiratory tracts; the ammonium chloride is an expectorant and enables sputum to be discharged easily through increase of sputum quantity, thereby facilitating removal of phlegm, enabling cheesy material and phlegm in tracheas to be diluted, dissolved and discharged out of the body, and keeping smooth breath. Through combination of the two medicines, the composition aims at pathogeny and also aims at symptomatic treatment, can effectively improve the cure rate, and reduces losses caused by respiratory disease characteristics.
US7056529 Vesicle comprises ATP and phospholipid; fusion proteins A vesicle comprises ATP and a phospholipid which is a stable vesicle former. The vesicle has a fusion rate of at least 20 vesicle fusions/second.
CN102525946A Method for preparing erythromycin thiocyanate gelatin microsphere preparation The invention discloses a method for preparing an erythromycin thiocyanate gelatin microsphere preparation. The method comprises the following steps of: forming water-in-oil (W/O) emulsion with mechanical stirring by using gelatin as a carrier, using liquid paraffin as an oil phase and using Span85 and Tween80 as a mixed emulsifier, cooling glutaraldehyde at a low temperature, performing cross linking and curing, and thus obtaining microspheres of 7 to 20 microns. In intravenous administration, after the microsphere suspension is injected through the vein, the microsphere suspension is in contact with a lung capillary network of which diameter is 3 to 11 microns and is effectively intercepted by the lung; and medicaments in the microspheres are slowly released, so that a stable and long-term effective concentration is obtained. The preparation is prepared by adopting an emulsification and condensation polymerization method; and the method is low in equipment requirements, low in preparation cost and easy to popularize and apply.
CN103690955A Ticagrelor-containing drug composition as well as preparation method and application thereof The invention relates to a drug composition of ticagrelor and a type II therapeutic agent, and a preparation method of the drug composition. The type II therapeutic agent is selected from one or more of rosuvastatin calcium, genistein, daidzein, dipyridamole, atorvastatin calcium, simvastatin, lovastatin, pravastatin sodium, pravastatin calcium, lovastatin, fluvastatin sodium, amlodipine, nifedipine, olmesartan medoxomi I, telmisartan, candesartan cilexetil, losartan potassium, irbesartan and ezetimibe. The invention further relates to an application of the drug composition in drugs, especially aspects of inhibiting or reversing atherosclerotic lipid plaques of artery blood vessels.
US20130344113 Iron Fortified Food Product and Additive The present invention relates to a food product which has been fortified in iron content, comprising a Fe3O4 sphere. The present invention also relates to an iron-containing additive for use in the above food product, in the form of a Fe3O4 sphere. The present invention further relates to a method for preparing the above food product, comprising the steps of adding or mixing the iron-containing additive in solid or dispersed form with the food product, wherein the iron-containing additive is in the form of a Fe3O4 sphere.
US20100152282 Use of double stranded rna hairpin duplexes in gene silencing A DNA polynucleotide is described herein having a modified sequence of a target gene, wherein any one type of nucleotide in the target gene sequence has been chemically modified to another type of nucleotide; and a complementary sequence of the unmodified target gene; wherein either one of the modified sequence or the complementary sequence is in a reverse orientation to the other sequence; and wherein the RNA sequence transcribed from the DNA polynucleotide forms a duplex between the modified sequence and the complementary sequence so that a long double stranded RNA (IdsRNA) duplex forms between the modified and complementary sequences with base pair mismatches where the nucleotides have been modified, the IdsRNA duplex being capable of inhibiting expression of the target gene. RNA polynucleotides and IdsRNA duplexes transcribed by the DNA polynucleotide are also described, as is a method for producing the IdsRNA duplexes. These IdsRNA duplexes can be used in gene silencing.
US20080287550 Sertraline hydrochloride form II and methods for the preparation thereof The present invention is directed to Form II of sertraline hydrochloride and novel methods for its preparation. According to the present invention, sertraline hydrochloride Form II may be produced directly form sertraline base or sertraline mandelate. It may also be produced from sertraline hydrochloride solvate and hydrate forms, and crystallized from new solvent systems. Pharmaceutical compositions containing sertraline hydrochloride Form II and methods of treatment using such pharmaceutical compositions are also disclosed.
US20120289557 Protein Synthesis Required for Long-Term Memory is Induced by PKC Activation on Days Preceding Associative Learning The present invention provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.
CN101717423A Alisol A derivative, pharmaceutical composition and use thereof The invention relates to an Alisol A derivative shown in the formula (I), a pharmaceutical composition, a preparation method and a use of the compound and the pharmaceutical composition for preparing anti-hepatitis B inhibitor and the anti-hepatitis B medicament.
WO2007017649A1 Heteroarylcarbamoylbenzene derivatives for the treatment of diabetes Compounds of formula (I) wherein R1, R2, R3 and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
EP0883608B1 Optical resolution of methylphenidate by 0,0'-bisaroyl tartaric acids Single isomer methylphenidate, selected from the d- and l-threo-enantiomers, has been obtained in purified form, to the extent of less than 2 % by weight of a contaminant selected from resolving agent and ritalinic acid. This is achieved by resolution of a mixture of enantiomers using an 0,0'-diaroyltartaric acid as resolving agent.
US20090270406 Combination Therapy for the Treatment of Urinary Frequency, Urinary Urgency and Urinary Incontinence This invention concerns compositions for the treatment of urinary frequency, urinary urgency and urinary incontinence comprising (R)-N-[4-[2-[[2-hydroxy-2-(pyridin-3-yl)ethyl]amino]ethyl]phenyl]-4-[4-(4-tri-fluoromethylphenyl)thiazol-2-yl]benzenesulfonamide and pharmaceutically acceptable salts thereof. In another aspect, this invention concerns combination therapy for urinary frequency, urinary urgency and urinary incontinence wherein one of the active agents is (R)-N-[4-[2-[[2-hydroxy-2-(pyridin-3-yl)ethyl]amino]ethyl]phenyl]-4-[4-(4-tri-fluoromethylphenyl)thiazol-2-yl]benzenesulfonamide and pharmaceutically acceptable salts thereof.
US20120294929 Method of diagnosing and treating cancer using b-catenin splice variants The invention relates to method and compositions for treating and diagnosing cancer, in particular β-catenin related cancers. In general, the methods include administering RNAi constructs. The invention further relates to methods of identifying CTNNB1 related cancer therapeutics.
US20080293774 Treatment of the Symptoms of Bladder Irritation Use of a compound corresponding to formula (I), for obtaining a medicinal product for use in the treatment of the symptoms of bladder irritation.
CN101167805B Use of medicinal composition containing lotus leaves and hypericum japonicum total flavone extraction in preparing medicine for hepatitis B virus The invention relates to a medicament complex which is prepared from total flavone extract of lotus leaf and hypericum japonicum thunb, and new usage for preparing anti-hepatitis B virus medicament. The total flavone of lotus leaf and hypericum japonicum thunb of the invention is total flavone extract which is separated and extracted from lotus leaf and hypericum japonicum thunb which grow in China. The complex of lotus leaf and hypericum japonicum thunb is separated and purified, tested by mass spectrum, 13C and 1HNMR, and proved to contain the following chemical components: quercetin, quercetin-3-O-beta-D-galactopyranose, isoquercetin, and kacmpferol and the like. The complex of total flavone extract is tested by in vitro cell model and in vivo animal model and proved to have strong activity of resisting hepatitis B virus and protecting liver. The complex of total flavone extract can be further prepared into anti-hepatitis B virus medicament and dosage forms can be capsules, tablets, granules, and injection and the like.
WO2005097138A3 Combinations comprising oxcarbazepine to treat affective disorders The present invention relates to the treatment of affective disorders by administration of pharmaceutical oxcarbazepine combinations.
WO2014150074A1 Compositions and methods for nucleic acid delivery The present invention provides, among other things, multilayer film coating compositions, coated substrates and methods thereof. In some embodiments, a structure includes a substrate; and a multilayer film coated on the substrate, wherein adjacent layers of the multilayer film are associated with one another via one or more non-covalent interactions, wherein the multilayer film comprises a first nucleic acid agent present at a loading density, and further wherein the multilayer film is characterized in that, when the structure is placed on a subject so that the multilayer film contacts cells, the first nucleic acid agent is released with a profile characterized by a feature selected from the group consisting of 1) being a burst-free release; 2) being a sustained release; and 3) exhibiting in vitro and/or in v/Vobiological effectiveness. The structure is in particular suitable for the local delivery of siRNA.
WO2014106623A1 C-terminal hsp90 inhibitors to treat pituitary adenomas The present invention relates to C-terminal HSP90 inhibitors, like silibinin, novobiocin and derivatives thereof, stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said compounds and its compositions have been identified as useful for the treatment of pituitary adenomas such as corticotroph adenomas, lactotroph adenomas, somatotroph adenomas and thyrotroph adenomas.
CN102746307A 1-N-benzyl allopurinol derivative as well as preparation method and application thereof The invention provides an allopurinol derivative shown in a formula I, as well as a preparation method and an application thereof. The allopurinol derivative can effectively inhibit tumor growth, and has a good antitumor effect; the allopurinol derivative can also effectively inhibit xanthine oxidase activity, can be used for gout treatment, and provides a new pharmaceutical option for clinicallytreating cancer and gout; and moreover, the preparation method of the compound is simple, is lower in cost, and has high yield and a good industrial application prospect.
CN1615821A Embolism agent The present invention dscloses a embolism agent for treating hemoptysis and hemostasis. The embolism agent has medicine for bacteriostasis and killing tuberle bacillus, and can embolize bleeding vessel caused by erosion of tubercule bacillus, treat local tuberculosis focus, stop bleeding and treat tuberculosis. In addition, the present invention has low cost.
EP1240328B1 Antigenic protein lppq of mycoplasma mycoides subsp. mycoides sc., its preparation and use The invention relates to protein LppQ of Mycoplasma mycoides subsp. mycoides SC, DNA encoding said protein, processes for the preparation of the protein and the DNA, a vector comprising the DNA, a host cell comprising the vector, use of the protein in immunological methods for the detection of M. mycoides subsp. Mycoides SC, use of the DNA in genetic methods for the detection of M. mycoides subsp. mycoides SC, use of the protein and DNA for preparing a vaccine against M. mycoides subsp. mycoides, processes for the immunological detection of antibodies directed to M. mycoids subsp. Mycoides SC and PCR process for the detection of M. mycoides subsp. mycoides SC, a monoclonal antibody specific for LppQ or parts thereof and a diagnostic kit for the detection of an infection with Mycoplasma mycoides subsp. mycoides SC.
US7183277 Alpha-((aryl or heteroaryl)ureido or carbamoyloxy)-N-heteroaryl amides; blood-coagulation factor Xa and VIIa inhibitors; synergistic mixtures with other antitumor agents or anticoagulants Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.
US20110207680 Administration of Glufosfamide For The Treatment of Cancer Administration of Glufosfamide alone and in combination with another anticancer agent is useful for the treatment of gall bladder cancer.
CN103012530A Preparation method of compound endecaphyllacins B and application thereof in preparation of anti-tumor drugs The invention discloses a preparation method of a compound endecaphyllacins B and an application thereof in the preparation of anti-tumor drugs. According to the preparation method, the compound endecaphyllacins B is obtained through preparative separation of aquilaria sinensis (Lour.) Gilg.) pericarps, has obvious anti-tumor activity and can be used for preparing the anti-tumor medicines. Therefore, the realization of the compound endecaphyllacins B provides a candidate compound for the research and development of the new anti-tumor medicines and a scientific basis for the development and utilization of aquilaria sinensis plant resources.
WO2012017555A1 Elastase inhibitor An elastase inhibitor contains raspberry extract and hydroxyproline as active ingredients, and optionally contains yeast extract.
US20100166886 Methods of treating the skin The invention features a method of (i) reducing the appearance of pores or oil on the skin and (ii) evening skin tone or smoothing skin by applying to an area of skin in need of such treatment a composition including an anti-acne agent, an antimicrobial agent, and a lactate.
US20120065267 Compositions including 3,5-l-t2 and methods of use thereof Compositions containing 3,5-L-T2 ((2S)-2-amino-3-[4-(4-hydroxyphenoxy)-3,5-diiodophenyl]propanoic acid) and methods for use thereof. Among other functions presented herein, 3,5-L-T2 can lower cholesterol via a mechanism that is independent of LDL receptor function. Disclosed compositions may include one or more additional active agents, such as, but not limited to, thyroid hormones other than 3,5-L-T2, cholesterol lowering agents, anti-diabetes agents, anti-hypertensives, vasodilators, inotropic agents, anti-coagulants, anti-anginals, anti-arrhythmics, leptin, leptin analogues, and adipokines, a vitamin and mineral composition. Disclosed methods include, but are not limited to, methods for treating hypercholesterolemia in a subject, and methods for treating at least one of metabolic syndrome, hypothyroidism, or thyroid suppression.
CN103520677A Hair-growing wine formula A provided hair-growing wine formula comprises the components in parts by weight: 1000-1300 parts of Chinese liquor, 10-13 parts of rhododendron molle, 5-6 parts of psoralea corylifolia, 11-14 parts of fresh ginger, 4-7 parts of kaempferia galangal, 9-12 parts of vatica mangachapoi, 4-6 parts of camphor, 12-15 parts of yerbadetajo herb, 4-6 parts of polygonum multiflorum, 8-10 parts of morinda officinalis, 4-7 parts of rhizoma atractylodis and 3-5 parts of cacumen platycladi. The hair-growing wine formula is an external-used hair-growing wine formula capable of preventing hair loss, growing and strengthening hair.
CN101002762A Application of galangin for treating irritable bowel syndrome, and its extraction method An application of the galangin in preparing the medicines for treating irritable bowel syndrome (IBS) is disclosed. The preparing process for extracting galangin features use of alcohol extracting-water deposition method to obtain coarse extract and use of macroreticular resin technique and glucosan gel technique to separate and purify it.
EP1140273B1 Device for locally delivering a drug in a body cavity A method of site-specifically delivering a therapeutic agent to a target location within a body cavity. The method comprises the steps of providing a medical device such as a catheter stent filter or vascular graft with a coating containing that agent. Introducing the medical device into the body cavity releasing a volume of the solution of therapeutic agent from the medical device by diffusion contacting the target site surface. In another embodiment, the present invention includes a system for delivering a therapeutic agent into a body cavity comprising a medical device injecting the agent via the needle.
CN103520217A Biological bactericide and application thereof A biological bactericide and application thereof relates to a biological bactericide and application thereof. The biological bactericide aims at solving the problems that conventional bactericides are harmful to human body because of contained chemical components. The biological bactericide is composed of 0.2-5 g/L of nisin, 1-15 g/L of EDTA disodium salt, 50-100 g/L of glycerin, 10-200 g/L of a hydrophilic solvent, 1-10 g/L of an edible organic acid, 0.01-0.5 g/L of essence the balance purified water. The biological bactericide is used for sterilizing hands, article surfaces and public places. The biological bactericide is nontoxic and innocuous to human body, is decomposed into amino acids utilized by human body after taken by a person, and causes no damage to human body. The biological bactericide is applicable to the field of bactericides.
CN101919846A Drug application of N2,N5-bi[2-(3,4-imethoxyphenyl)ethyl]-2,5-pyridine carboxamide The invention discloses application of a micromolecular compound with HIV (Human Immunodeficiency Virus) resisting activity to preparing drugs for resisting AIDS, relating to the field of biomedicine. The world health organization (WHO) and governments around the world highly pay attention to AIDS called as present pestilence and super cancer, however, so far, effective drugs capable of curing the AIDS do not exist. The invention provides application of N2,N5-bi[2-(3,4-imethoxyphenyl)ethyl]-2,5-pyridine carboxamide to preparing the drugs for resisting the AIDS. The N2,N5-DI[2-(3,4-imethoxyphenyl)ethyl]-2,5-pyridine carboxamide has the capability of inhibiting the replication of HIV-1 virus and is designed by aiming at cell target points without easily generating drug resistance as well as is suitable for the medication demands of the AIDS patients for life.
US20080033049 Hydroxy-Biphenyl-Carbaldehyde Oxime Derivatives and Their Use As Estrogenic Agents This invention provides estrogen receptor modulators having the structure: wherein R1 to R6 and R8 are as defined in the specification; or a pharmaceutically acceptable salt thereof.
US6881739 Use of cortisol antagonists in the treatment of heart failure The present invention relates to the use of a cortisol antagonist in the manufacture of a medicament for the treatment of heart failure as well as to a method of treating heart failure which comprises administration of a cortisol antagonist and to a product containing (a) a cortisol antagonist and (b) a second drug as a combined preparation for simultaneous, separate or sequential use in the treatment of heart failure or in improving cardiac function and reducing exercise intolerance.
CN103536922A Application of acyl-coenzyme A: cholesterol acyltransferase-2 (ACAT2) inhibitor in liver cancer growth inhibition The invention relates to application of an acyl-coenzyme A: cholesterol acyltransferase-2 (ACAT2) inhibitor in liver cancer growth inhibition. Concretely, the inhibition of the activity of the ACAT2 can effectively inhibit the growth of human liver cancer cells and transplanted tumors respectively in cellular and animal levels, and the inhibitory effect is generated through accumulating intracellular cholesterol metabolites by blocking the secretion and excretion of ACAT2-mediated cholesterol metabolites. The accumulation of the cholesterol metabolites has effects on promoting the apoptosis of liver cancer cells and inhibiting the growth of liver cancer; the excretion of the cholesterol metabolites can remove the inhibitory effect.
WO2008004944A1 Novel crystalline form ii The present invention relates to 6-(4-{[(benzylsulfonyl)amino]carbonyl}piperidin-1-yl)-5-cyano-2-methylnicotinic acid isopropyl ester, form II, to a process for preparing such compound, to its utility as P2Y12 inhibitor and as anti-thrombotic agent etc, its use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing it.
WO2014124487A1 Ligand binding molecules and uses thereof The present invention is directed to ligand binding molecules and uses thereof to modulate angiogenesis and/or lymphangiogenesis.
EP1272218B1 A pharmaceutical composition for treatment of acute, chronic pain and/or neuropathic pain and migraines Pharmaceutical compositions are disclosed for the treatment of acute, chronic and/or neuropathic pain. The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotine receptor partial agonist and an analgesic agent and a pharmaceutically acceptable carrier. The analgesic agent is selected from opioid analgesics, NMDA antagonists, substance P antagonists, COX 1 and COX 2 inhibitors, tricyclic antidepressants (TCA), selective serotonin reuptake inhibitors (SSRI), capsaicin receptor agonists, anesthetic agents, benzodiazepines, skeletal muscle relaxants, migraine therapeutic agents, anti-convulsants, anti-hypertensives, anti-arrythmics, antihistamines, steroids, caffeine, and botulinum toxin. The method of using these compounds and a method of treating acute, chronic and/or neuropathic pain and migraine in a mammal including a human is also disclosed.
US20130053438 Pharmaceutical compositions comprising lignans and their derivatives for the medical management of angiogenesis and hypovascularity The present invention relates to a pharmaceutical composition for stimulating angiogenesis and/or the treatment or prevention of hypovascularity and/or the prevention and/or treatment of an angiogenic disorder/disease, whereby the composition comprises specific compounds which may be obtained from Leontopodium alpinum Cass, (Edelweiss). These compounds relate to lignan compounds as shown in herein disclosed formula I. A preferred compound in this context is leologin—IUPAC name [(2S,3R,4R)-4-(3,4-dimethoxybenzyl)-2-(3,4-dimethoxyphenyl)tetxahydrofuran-3-yl]methyl (2Z)-2-methylbut-2-enoat], and even more particularly 5-methoxy-leoligin (IUPAC name: [(25,3R,4R)-4-(3,4-dimethoxybenzyl)-2-(3,4,5-trimethoxyphenyl)tetrahydrofuran-3-yl]methyl-(2Z)-2-methylbut-2-enoat) and derivatives thereof. Corresponding means and methods in respect of medical uses of these compounds are described. The compounds provided herein may particularly be useful in the treatment of wound healing, in particular traumatic wounds (like, but not limited to surface and skin wounds), non-diabetic retinopathy, vascular obliteration. The compounds derived from Leontopodium alpinum Cass. (Edelweiss) as described herein are also useful in the re-vascularization of tissue after amputation as well during or after transplantation of tissues or organs. These compounds are also useful in the medical intervention of arterio- and veno-microvasculopathy of blood vessels, in particular retinal microvasculopathy, arterio- and veno-microangiopathy that preferably cannot be treated by surgery, in ischemic diseases or ischemic disorders or in the treatment or prevention of necrosis/necrotic events, in particular of ischemic diseases or necrosis/necrotic events that cannot be treated by surgery. These compounds may also be used in the treatment or prevention of stable angina abdominalis, vascular dementia, impotence or penile dysfunction and the like and they may be employed in the reactivation of necrotisising tissue or in the reactivation of hibernating tissue.
WO2013028501A1 Combination therapy with nitrated lipids and inhibitors of the renin-angiotensin-aldosterone system The present technology provides compositions and methods for treating chronic kidney disease, end-stage renal disease, or diabetic nephropathy. The compositions comprise a nitrated lipid and an inhibitor of the renin-angiotensin-aldosterone system. The methods comprise administering a nitrated lipid in combination with an inhibitor of the renin-angiotensin-aldosterone system to a subject in need thereof, in an amount effective to treat diabetic nephropathy, chronic kidney disease, and/or end-stage renal disease. The use of a nitrated lipid with an inhibitor of the renin-angiotensin-aldosterone system exhibits a synergistic effect in treating chronic kidney disease and diabetic nephropathy.
US20120087893 Combinations of a hcv inhibitor such as bicyclic pyrrole derivatives and a therapeutic agent The present invention is directed to a combination product for treating or ameliorating hepatitis C virus (HCV) infection or disorders or symptoms associated therewith in a subject in need thereof comprising, a HCV inhibitor and one or more therapeutic agents selected from either or both a HCV protease inhibitor and one or more different therapeutic agents administered in combination in an effective amount to the subject.
US20100029672 Method of treating liver disease Treating diseased or damaged tissue, particularly the liver, using stem cells. The hepatic stem cell population of a subject suffering from disease or damaged tissue can be expanded by administering at least one regulator of the sympathetic nervous system. The regulator can be an adrenoceptor agonist or antagonist, adrenoceptor antagonists, prazosin, being particularly preferred. The invention also includes the use of agents which mobilize stem cells in the manufacture of medicaments for the treatment of diseased or damaged tissue.
CN102716168A Rifaximin-containing preparation for preventing and treating dairy cow mastitis during dry period and method for preparing rifaximin-containing preparation The invention relates to a rifaximin-containing preparation for preventing and treating dairy cow mastitis during the dry milk period, which comprises the main active ingredients of rifaximin and dandelion plant extracts, the auxiliary ingredients of thickening agent poloxamer 407, a viscosity modifier isopropyl myristate, an antioxidant butylated hydroxytoluene (BHT) and a solvent medical castor oil. The rifaximin-containing preparation can be used as an udder injectant for preventing and treating the dairy cow mastitis during the dry milk period, which is caused by staphylococcus aureus, staphylococcus epidermidis, streptococcus, enterococcus, corynebacterium, Escherichia coli, salmonella, shigella and bacteroides.
US20120252891 Vanilloid Fatty Hydroxamates as Therapeutic Anti-inflammatory Pharmaceuticals Three unique subtypes of N-hydroxyamides and N-hydroxycarbamates containing both the vanilloid moiety (4-hydroxy-3-methoxybenzyl) and a lipophilic aliphatic moiety. Also disclosed are direct syntheses of these vanilloid fatty hydroxamates. The compounds possess inhibitory activity against the enzymes fatty acid amide hydrolase (FAAH) and matrix metallo-proteinase 9 (MMP-9). In addition, these substances bind to the calcium channel protein TRPV1 and inhibit vesicant-induced inflammation in skin and cornea. The compounds have utility in treating topical or systemic inflammatory processes in the skin and/or eye.
US20110059954 Cgrp antagonists The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
US20070292355 Alcohol-free drug or cosmetics carrier mixture of water, hydrophobic solvent, surfactant and gelling agent; oil in water emulsions Anti-infective foamable composition and kits include a foamable carrier; a therapeutically safe and effective concentration of an anti-infective agent; an augmenting agent selected from the group consisting of a keratolytic agent and a skin penetration enhancer; and a propellant. The composition is housed in a container and upon release is expandable to form a breakable foam. The foamable carrier is selected to generate a foam of good or excellent quality in the presence of the augmenting agent and anti-infective agent. Methods for treating, alleviating or preventing a disorder of the skin, a body cavity or mucosal surface, wherein the disorder involves a fungal, bacterial or viral infection as one of its etiological factors, is described.
US20090203732 Thiazolones for Use as P13 Kinase Inhibitors Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones.
CN1683303A Novel use of 3, 4-dihydroxy-benzene formaldehyde and its derivatives in treating hypatitis B and virus infectious diseases The present invention relates to the application of substituted derivative of protocatechuic aldehyde, ester derivative of protocatechuic aldehyde, acetal derivative of protocatechuic aldehyde, amide derivative of protocatechuic aldehyde, and Schiff base derivative of protocatechuic aldehyde in treating hepatitis B and other viral infectious diseases; and the said medicine compound or their composition may be used through combination with antiviral neucleoside analog medicine in treating hepatitis B and other viral infectious diseases.
US20120282338 Extended Release Formulation The invention is directed to an extended release formulation comprising pramipexole or a pharmaceutically acceptable salt thereof.
CN103284961A Preparing method of cobamamide freeze-drying formulation for injection The invention relates to a cobamamide freeze-drying formulation for injection and a preparing method thereof. According to a specific amount, the amount ratio of adenosylcobalamin, mannitol and water for injection is 0.52 g: 25 g: 500 ml. The preparing method comprises: operating in a dark environment, weighing mannitol according to a prescribed amount, adding the water for injection in an amount of about 90%, then stirring to achieve complete dissolution, adding cobamamide, and stirring to achieve complete dissolution; adding the water for injection to the full amount, stirring evenly, adding activated carbon in a preparation amount of 0.02% (W/V), and fully stirring; performing coarsely filtered decarburization of the obtained solution, then performing refined filtration with a 0.22 [mu]m microporous filtering membrane, determining the content, and calculating a package amount; sub-packaging; and performing freeze drying to obtain the final product. The method is simple in operation, has no need of any additional stabilizers and inert gas for protection, and has high product stability.
WO2008092873A1 Glyt1 transporter inhibitors and uses thereof in treatment of neurological and neuropsychiatric disorders Compounds of formula (I) or a salt thereof are provided:(I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R21 and m are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further discloses pharmaceutical compositions and combinations comprising the compounds.
CN1732927A Orally administered formulation of mitiglinide calaium hydrate The invention discloses a Mitiglinide oral preparation, which is prepared from Mitiglinide as reactive component through right preparing procedures, and is made into the forms of common oral administration tablet, dispersible tablet, thin film dressed tablet, orally disintegrating tablet, enteric coated tablet, slow release capsule, rapid release capsule, controlled release capsule, hard gelatin capsule, enteric-coated capsule, and slow release capsule.
US20080249064 plant extract polygalactomannans for use in cosmetic, treating aging of the skin, anti-wrinkle and smoothing properties The object of the invention is an active principle derived from a powder of alfalfa seeds (Medicago sativa) permitting counteracting, in a manner similar to retinol, the phenomenon of extrinsic aging of the skin, with anti-wrinkle and smoothing properties. The invention also covers the active principle, the procedure of obtaining the same, and the compositions including it.
CN101390869B Use of high-purity forsythin in preparing bacteriostasis, antivirus medicine The invention belongs to the medical technical field and discloses the application of high-purity in the preparation of antibacterial medicine, antiviral medicine and other medicines. The invention proves the antipyretic, anti-inflammation, immunity enhancement, antibacterial and anti-virus effects of high-purity forsythiaside through the following experiments: (1) the experiment that high-purityforsythiaside has antipyretic effect on fever rats; (2) the experiment that high-purity forsythiaside inhibits xylene-induced mice ear edema, xylene-reduced capillary permeability of mice; (3) the experiment that high-purity forsythiaside increases carbon clearance ability of mice and increases the lymphocyte transformation rate; (4) the experiment that high-purity forsythiaside has vitro anti-influenza A type virus effect and in-vivo anti-respiratory syncytial virus effect; (5) the experiment that high-purity forsythiaside has vitro inhibition effects on beta-hemolytic streptococcus, staphylococcus aureus, streptococcus viridans and staphylococcus epidermidis.
WO2009044439A1 Composition for preventing or treating liver disease It is intended to provide a composition for preventing or treating liver disease including liver cancer, which has no adverse effect and is easily taken, and a food or food material having the composition blended therein. A special salt, sale de tierra, is used as an active ingredient of the composition for preventing or treating liver disease. The sale de tierra is obtained by bringing a naturally occurring ion exchanger such as zeolite (mordenite) into contact with an aqueous sodium salt solution, an aqueous potassium salt solution, an aqueous calcium salt solution, an aqueous magnesium salt solution, ammonia water, an aqueous ammonium salt solution, an aqueous inorganic acid solution, an aqueous organic acid solution, sea water, salt lake water or hot spring water to elute components contained in the naturally occurring ion exchanger through ion exchange and subsequently separating the eluate from the naturally occurring ion exchanger. Further, by blending the composition, the food or food material for preventing or treating liver disease is prepared.
DE102007030495A1 Use of creatine containing preparation e.g. for improving memory, retentivity, long-term memory and for preventing mental fatigue condition, comprising e.g. Ginkgo biloba, ginseng and niacin Use of a creatine containing preparation for improving memory, retentivity, long-term memory and for preventing mental fatigue conditions, comprising e.g. at least a further physiologically effective component of the series Ginkgo biloba, ginseng, taiga root, yam root, lecithin, choline, phosphatidylserine, dimethylamino ethanol, acetyl choline, acetyl-L-carnitine, glutathione, glutamine, cysteine, vitamin A, E, B1, B2, B6, B12, folic acid, pantothenic acid and/or zinc, is claimed. Use of a creatine-component containing preparation for improving memory, retentivity, long-term memory and for preventing mental fatigue conditions, comprising at least a further physiologically effective component of the series Ginkgo biloba, ginseng, taiga root, yam root, lecithin, choline, phosphatidylserine, dimethylamino ethanol, acetyl choline, acetyl-L-carnitine, glutathione, glutamine, cysteine, vitamin A, E, B1, B2, B6, B12, E, niacin, biotin, folic acid, pantothenic acid, zinc, manganese, selenium, magnesium, coenzyme Q10, glucose, colostrum, synephrine, octopamine, caffeine, theophylline, alpha -linolenic acid, eicosapentaenoic acid, omega-3-fatty acid, piracetam, aniracetam, memantine, pyritinol, galantamine, vinpocetin, pangamic acid and/or optionally organic or inorganic salts and/or optionally esters, is claimed. - ACTIVITY : Nootropic; CNS-Gen; Cerebroprotective. - MECHANISM OF ACTION : None given.
CN101972230A Pirfenidone for suspension and preparation method The invention provides a pirfenidone for suspension and a preparation method thereof, which belong to the technical field of pharmacy and are used for solving the problem of bioavailability of pirfenidone. The product mainly consists of a primary pharmaceutical pirfenidone and auxiliary materials and has the advantages of high pharmaceutical solubility, stable chemical property, good taste, convenient administration and high obedience of patients.
CN101347450A Chondroitin sulfate in situ forming eye gel The invention discloses a chondroitin sulfate forming gel for eye use and a preparation method thereof. 1,000ml chondroitin sulfate forming gel for eye use of the invention contains 10 to 40g of chondroitin sulfate, 0.05 to 1g of antiseptic, 1.0 to 7.5g of osmoregulator, 30 to 150g of gel matrix and the rest of acid-base buffering agent and injection water. The invention, with the optimization of auxiliary materials and the improvement of process, enriches the dosage forms of chondroitin sulfate, greatly extends the staying time in eyes of the medicine and improves the curing effect without adverse stimulus responses.
CN103520190A High-energy substance for preventing and treating neurodegenerative disease of old people and medical application of substance The invention relates to a high-energy substance for preventing and treating a neurodegenerative disease of old people. The high-energy substance comprises one or more of compounds and derivatives of the compounds of phosphoenolpyruvic acid, creatine phosphoric acid, acetyl coenzyme A, adenosine triphosphoric acid, L-carnitine, s-adenosylmethionine, guanosine triphosphate, cytidine triphosphate, pyrophosphoric acid, 1,3-diphosphoglycerate and succinyl coenzyme A. The high-energy substance has the benefits as follows: the high-energy substance is used for treating the neurodegenerative disease of the old people, particularly the aged population, so as to delay and prevent dementia; and the high-energy substance is proved to be a novel medicine which is reasonable, safe and economical and used for treating the neurodegenerative disease, particularly senile dementia.
US20080317739 Method for Treating Skeletal Disorders Resulting from Fgfr Malfunction The invention provides materials, reagents, systems, and methods for identifying agents useful for treating diseases resulting from abnormal (e.g., excessive) FGF receptor signaling. The invention also provides (therapeutic) agents thus identified, and methods of using such agents in treating such diseases. In certain embodiments, the invention relates to the treatment of various craniofacial disorders, or Craniosynostosis, that result from FGFR (e.g. FGFR2) malfunction, such as Crouzon, Apert, Jackson-Weiss, Pfeiffer Syndromes, Crouzon+acanthosis nigricans, Beare-Stevenson cutis gyrata, and non-syndromic craniosynostosis (NS). The methods comprise administering to the individuals a therapeutically effective amount of an inhibitor of the FGFR2c-FRS2 signaling. The inhibitor inhibits signaling by antagonizing FGFR2c-FRS2 interaction, inhibiting the expression and/or subcellular localization of wild-type or mutant FGFR2c and/or FRS2, inhibiting the kinase activity of FGFR2c (e.g. for autophosphorylation and/or phosphorylation of FRS2), and/or inhibiting downstream signaling of FRS2 (such as Sos-Ras-MAPK, Shp2, and/or Gab 1-PI3K pathways).
EP2051958A1 Phenyl-prenyl-ether derivatives for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders The present invention is related to a family of phenyl-prenyl-ether derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or 5 Parkinson's Disease. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder.
US20080249130 Oral dosage forms; antiproliferatives, anticholesterol agents; lipid metabolic disorders; myocardial infarction, stroke, restenosis, atherosclerosis Compounds represented by formula (I): are inhibitors of gut microsomal triglyceride transfer protein. Such compounds are useful in treating diseases or conditions such as diabetes and obesity, along with patients are risk for developing such diseases or conditions.
EP1575953A1 Anhydrous crystalline form of valacyclovir hydrochloride Valacyclovir hydrochloride in anhydrous crystalline form having substantially the following d-spacing pattern (in angstroms) (see (I)).
US20080269210 Using 1-(4-((2-(2-aminopyrimidin-5-yl)-4-morpholinothieno(3,2-d)pyrimifin-6-yl)methyl)piperazin-1-yl)-2-(methylsulfony)ethanone; lipid kinase inhibitor; anticancer agents Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
CN1985864A Medicine composition of glycyrrhizic acid or its salt, ginseng and glossy ganoderma The present invention belongs to the field of medicine technology, and is especially one medicine composition for treating hepatitis and its preparation process and use. The medicine composition consists of glycyrrhizic acid or its pharmaceutically acceptable salt 4-800 weight portions, ginseng 250-16000 weight portions, and glossy ganoderma 500- 20000 weight portions. It may consist of glycyrrhizic acid or its pharmaceutically acceptable salt, the extract of ginseng and the extract of glossy ganoderma. It may be prepared into different forms. The medicine composition has the synergistic effect of the components, high stability, high effect and wide application.
US20050143360 dysmenorrhea; e.g. celecoxib and ethinyl estradiol and levonorgestrel; side effect reduction as lower doses possible The present invention provides methods for the treatment and prevention of dysmenorrhea in a woman using a combination of a cyclooxygenase-2 inhibitor and sex steroids.
CA2381187C Intravenous carnitine for the treatment of chronic uraemic patients undergoing periodical dialysis The method for the treatment of chronic uraemic patients undergoing periodical dialysis is useful for preventing and/or treating carnitine deficiency in patients with end stage renal disease who are undergoing dialysis. The method according to the present invention comprises administering an effective dose of carnitine intravenously into the venous return line after each dialysis session.
US20120148667 Bioresorbable fillers constituted by phospholipid liposomes and hyaluronic acid and/or the derivatives thereof The present invention describes a new bioresorbable filler constituted by hyaluronic acid and/or the derivatives thereof structured with/in phospholipid liposomes, which increase the residence time of the starting polymer in situ. Said fillers described herein are substantially intended to increase the soft tissues in aesthetic surgery and dermocosmetics for the correction of mild to medium defects, but because of their special characteristics they can also be used in other fields of application.
CN103764134A Use of organic compound for the treatment of noonan syndrome The use of a MEK inhibitor compound of Formula (I), as defined herein, or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of Noonan Syndrome, a method of treating a warm-blooded animal, especially a human, having Noonan Syndrome, comprising administering to said animal a therapeutically effective amount of a MEK inhibitor compound of Formula (I), as defined herein, or a pharmaceutically acceptable salt thereof; and to a pharmaceutical composition and a commercial package comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and a package insert or other labeling including directions for treating Noonan Syndrome.
CN1788729A Pharmaceutical composition containing nevirapine and valproic acid or its salt The present invention is the therapeutic composition of Nevirapine and valproic acid or its salt. The medicinal composition consists of Nevirapine 0.1-95 wt%, valproic acid or its salt 1.0-95 wt% and medicinal supplementary material 4-98.9 wt%. Each unit of the medicine preparation includes Nevirapine 100-300 mg, valproic acid or its salt 50-500 mg and pharmaceutically acceptable supplementary material in 15-40 wt% preferably. The medicinal composition is used in treating HIV infection, especially treating AIDS or ARC of AIDS. The medicinal composition of Nevirapine and valproic acid or its salt is superior to anti-AIDS medicine Nevirapine and valproic acid or its salt, which can not 'awake' HIV inside CD4+ cell in dormancy state, and has relatively low cost.
WO2009000038A1 Combination methods and compositions for treatment of neuropathic pain The present invention relates generally to the field of pain management, and in particular, the management of neuropathic pain. The present invention further provides methods and compositions that treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms of neuropathic pain without inducing overt sedation. The present invention also contemplates combination therapy using one or more NK antagonists in combination with one or more compounds which decrease or inhibit neuronal excitation in the treatment of pain in association with the treatment of a particular disease condition or pathology.
US7943174 Controlled release hydrocodone formulations A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.
CN103099808A Application of para-di-n-propylamine sulfonyl benzoic acid to veterinary medicines The invention relates to an application of para-di-n-propylamine sulfonyl benzoic acid to veterinary medicines, and in particular relates to combined utilization of para-di-n-propylamine sulfonyl benzoic acid and penicillin medicines or fluoroquinolones medicines. The application has the advantages that the therapeutic effect of certain therapeutic medicines is enhanced, the purpose that a small amount of antibiotics is used in animal production is achieved, the occurrence of drug resistant strains is prevented or slowed in the animal production, and moreover, the functions of prolonging the administration time and reducing the cost can be realized.
US20100047292 Methods of processing microparticles and compositions produced thereby A method for processing multi-phasic dispersions is provided. The method comprises providing a multi-phasic dispersion including dispersed and continuous phases, positioning the multi-phasic dispersion within a chamber capable of being pressurized, pressurizing the chamber with a first gas to a pressure less than the supercritical pressure of the gas, and contacting the multi-phasic dispersion with the first gas.
CN102641370A Pharmaceutical composition ointment for treating rhinitis The invention discloses a pharmaceutical composition ointment for treating rhinitis, which is characterized by comprising the following raw materials: siberian cocklour fruit, biond magnolia flower, scutellaria, phellodendron, coptis, cortex dictamni, gardenia, mint, ash bark, honeysuckle, lemonfragrant angelica root, cicada slough, radix bupleuri, asarum, borneol, camphor, centipedes, potassium sorbate and vaseline.
CA2340238C Improved stability for injection solutions A primary package containing a low molecular weight peptide-based thrombin inhibitors which package is sealed with a rubber stopper or plunger containing bromobutyl rubber.
CA2444031C 3,4-di-substituted cyclobutene-1,2-diones as cxc-chemokine receptor ligands There are disclosed compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
US20120214771 Compositions for treatment of cardiometabolic disorders The present invention provides for methods of preventing or improving cardiometabolic disorders/metabolic disorders, compositions and pharmaceutical compositions comprising therapeutically effective amount of therapeutic phospholipid compositions and therapeutically effective amount of one or more lipid modifying agents, including statins.
CN102579642A Compound grapefruit oil nanoemulsion oral liquid for losing weight and preparation method thereof The invention discloses compound grapefruit oil nanoemulsion oral liquid for losing weight. The oral liquid consists of the following raw materials in percentage by mass: 24.5 to 38.6 percent of surfactant, 0.2 to 5.8 percent of oil, 2.2 to 15.5 percent of grapefruit oil, 1.8 to 10.5 percent of synephrine, 0.1 to 6.2 percent of seabuckthorm seed oil and the balance of distilled water; and the sum of the mass percentage of the raw materials is 100 percent. The compound grapefruit oil nanoemulsion oral liquid has the effects of promoting cell growth, promoting steatolysis, expelling toxin and keeping young, increasing the discharge of urine, resisting bacteria and diminishing inflammation and promoting digestion. When used for female weight loss, health care and beauty maintenance, the nanoemulsion oral liquid is safe, high in stability and convenient to popularize and apply, does not have side effects, and has an obvious effect and high content of active ingredients.
US20080161308 e.g. 4-[6-(2-cyclohexylethoxy)-3-oxoindan-5-yloxy]butanoic acid; peroxisome proliferator-activated receptor (PPAR) gamma agonist; antiinflammatory, antidiabetic agent; dyslipidaemia, atherosclerosis, insulin resistance Compounds of the formula (I): in which A, R1, R2, X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.
CN103127069A Application of Eryngiolide A in medicines treating acute renal failure The invention relates to novel medical application of Eryngiolide A, namely, application of the Eryngiolide A in preparing medicines treating acute renal failure. The application of the Eryngiolide A in preparing medicines treating acute renal failure is made public for the first time, due to the fact that matrix type is brand novel, besides, the Eryngiolide A has an unexpectedly high acute renal failure inhibitory activity, the possibility that inspiration is obtained from other compounds does not exist, and the Eryngiolide A possesses outstanding substantial characteristics, meanwhile, significant progress is obviously achieved by the application of the Eryngiolide A in resisting acute renal failure.
US20050163707 Radio labelled monoclonal antibody human milk fat globule1, binds selectively to polymorphic epithelial mucin; Taxotere chemotherapeutic agent; administered in combination The invention relates to a therapeutic system comprising (i) a radiolabelled antibody, which binds selectively to polymorphic epithelial mucin (PEM) such as the monoclonal antibody HMFG-1, and (ii) a chemotherapeutic agent, such as Taxotere®. The radiolabelled antibody and chemotherapeutic agent are administered in combination with one another to produce a synergistic therapeutic effect.
CN103211790A Tamsulosin hydrochloride film-controlled slow-release pellet capsule The invention relates to a tamsulosin hydrochloride film-controlled slow-release pellet capsule. A slow-release film of the tamsulosin hydrochloride film-controlled slow-release pellet utilizes Eurdragit NE30D and HPMC E5 as film-formation materials. A pellet core of the tamsulosin hydrochloride film-controlled slow-release pellet contains sodium carboxymethyl starch having high expansibility, and also contains pharmaceutically-acceptable common excipients for the slow-release pellet, wherein preferably, the excipients comprise microcrystalline cellulose and lactose as fillers, and polysorbate 80 as a solubilizer; and the pellet core comprises 5 to 20wt% of sodium carboxymethyl starch. The slow-release film comprises Eurdragit NE30D, HPMC E5 and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit NE30D to HPMC E5 to talcum powder is 30: 2: 4 and a film weight increasing ratio is in a range of 19 to 36%. The tamsulosin hydrochloride film-controlled slow-release pellet comprises the pellet core containing sodium carboxymethyl starch having high water expansibility and thus after absorbing water, the tamsulosin hydrochloride film-controlled slow-release pellet obviously expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the tamsulosin hydrochloride film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.
US20120270847 Novel carbamate amino acid and peptide prodrugs of opiates and uses thereof Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid pro-drug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
WO2014065575A1 4,5-dihydro-1h-pyrazole derivative or salts thereof, and pharmaceutical composition comprising same The present invention provides 4,5-dihydro-1H-pyrazole derivative or pharmaceutically acceptable salts thereof, a method for preparing same and a pharmaceutical composition comprising same. The 4,5-dihydro-1H-pyrazole derivative or pharmaceutically acceptable salts thereof may effectively increase LXR transcriptional activity, and therefore, can be usefully applied to the prevention and treatment of cholesterol metabolism disorders including cholesterol gallstones, hyperlipidemia, coronary sclerosis and atherosclerosis.
US20080269233 Piperidinoyl-Pyrrolidine and Piperidinoyl-Piperidine Compounds The present invention relates to a class of compounds of general formula (I) and the salts, hydrates, solvates, polymorphs and prodrugs wherein n, R6, R7 and R10 are as defined herein and especially to MCR4 agonist compounds of formula (I), to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
CN101040843A Solid tumor resisting release agent including nimustine and the intensifier A nimustine slow release injection for treating solid cancer comprises slow release finding and nimustine, or the combination of nimustine and relative booster (pidorubicin, osaliplatinum, adriablastina, amethopterin or the like). The viscidity of slow-release injection is 10-650cp (20-30Deg. C). The anti-cancer effective component can be made into slow release plant agent. The slow release finding substantially comprises macromolecule polymer with biological soluble degradable and absorb property, which can slow release the anti-cancer effective component to cancer part in the degradation process, significantly reduce general reaction and hold effective drug density on cancer. The anti-cancer compound can be arranged part of cancer to reduce the general toxicity reaction, selectively improve the drug density locally, and strengthen the effect of non-surgery treatments as chemotherapy, and radiation therapy or the like. The solid cancer comprises glioma, lung carcinoma, intestinal cancer, breast cancer or the like.
CN101366701A N, N-dimethyl collagen sugar-2, 6-diisopropyl benzene ester salt injection The invention provides N, N-dimethyl glycine-2, 6-diisopropyl phenyl ester salt injection. The injection comprises the following raw materials: N, N-dimethyl glycine-2, 6-diisopropyl phenyl ester salt, PH regulator, isosmotic regulator, medicinal cyclodextrin of alpha-cyclodextrin, beta-cyclodextrin or gamma-cyclodextrin, wherein the N, N-dimethyl glycine-2, 6-diisopropyl phenyl ester salt is amounted to propofol; the specification of a single dose is between 10 and 1,000 milligrams; the PH value is in the range of between 2.5 and 7; the dose of the isosmotic regulator is set according to adjusting the osmotic pressure of a solution to the range of between 280 and 310mmol/L of the osmotic pressure of normal body fluid of human body when the injection is prepared; and the dose of an auxiliary material accounts for 5 to 10,000 percent of the weight of the N, N-dimethyl glycine-2, 6-diisopropyl phenyl ester salt. Through adding the medical auxiliary material which can reduce simulation, the N, N-dimethyl glycine-2, 6-diisopropyl phenyl ester salts injection can not only remove the side effect possibly produced by 2, 6-diisopropyl phenol emulsion but also avoid the simulation to blood vessels.
US20110053894 Broad Spectrum Antiviral and Methods of Use A method for the prevention or treatment of Influenza virus infection or Adenovirus infection by administering an effective amount of a compound of Formula (I), Formula (II), or similar compound to an individual in need is provided.
EP2083812A1 Use of arginase inhibitors in the treatment of asthma and allergic rhinitis The present invention relates to the use of an arginase inhibitor for the preparation of a medicament for the prophylactic maintenance therapy of an asthmatic or allergic patient by preventing obstruction of upper and lower airways, in particular allergen-induced bronchial obstruction and/or airway hyperresponsiveness. The patients are either asthmatic or have allergic rhinitis. Preferably, the arginase inhibitor is 2 (S) -amino-6-boronohexanoic acid (ABH).
CN103664726A Deuterated bimatoprost or derivative thereof and preparation method and application of deuterated bimatoprost or derivative thereof The invention relates to deuterated bimatoprost or a derivative thereof. A novel deuterated drug compound is formed by substituting an isotopic nuclide deuterium atom (D) for a hydrogen atom (H) contained in a bimatoprost structure and changing the chemical molecular structure and bond energy of the bimatoprost structure. The deuterated drug compound can be used for pharmacokinetic research, achieves obviously enhanced drug property and reduces the toxic side effect of a drug. The invention also relates to a preparation method and application of the deuterated bimatoprost or the derivative thereof.
CN101596279A Drug combination for reducing blood sugar and lipid levels and treating diabetes A drug combination for reducing blood sugar and lipid levels and treating diabetes comprises Ophiopogon japonicus (L.f) Ker-Gawl., Polygonatum sibiricum Red, vitamin A, beta-carotene, vitamin B complex, vitamin C, vitamin D, vitamin E, major elements such as calcium and magnesium, and trace elements such as zinc, selenium, chromium and molybdenum. The drug combination is mainly suitable for the population suffering from high blood sugar and lipid levels and diabetes, has good effects on reducing blood sugar and lipid levels and treating diabetes and can be taken for long term or according to the courses of treatment.
CN103319438A 4-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivative and its preparation method and application The invention relates to the technical field of medicine. The invention provides a 4-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivative and its pharmaceutically acceptable salt. The structural general formula of the compound is as shown in the formula I. The invention also provides a preparation method of the above 4-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivative and its pharmaceutically acceptable salt and an application in the preparation of a topoisomerase inhibitor or antitumor drug.
US20110112128 Method of treating ileus by pharmacological activation of cholinergic receptors A method of treating ileus in a subject by administering to the subject an effective amount of a pharmacological agent that increases the activity of cholinergic receptor in a subject. Examples of pharmacological agents are brain muscarinic agonist, cholinergic agonist or cholinesterase inhibitor. The methods of the present invention can be used to treat ileus caused by abdominal surgery, or administration of narcotics or chemotherapeutic agents such as during cancer chemotherapy.
CN1981740A Topical composition for delivery of salicylate esters or salicylate salts The present invention provides a self-emulsifiable composition and a stable topical emulsion comprising same, which comprises salicylate esters, oils and surfactants and which does not require organic solvents. The invention also provides methods for manufacturing the compositions. The topical compositions of the invention can be used to enhance delivery of salicylate esters and are useful in the prevention and treatment of pain and inflammation.
EP2686429A1 Compositions, process of preparation of said compositions and method of treating inflammatory diseases The present disclosure describes a composition and a kit having a plurality of compounds for use in the treatment of inflammatory joint diseases and chronic inflammatory connective tissue diseases, such as Rheumatoid Arthritis (RA). The disclosure also relates to a process of obtaining the composition and the method oftreating diseases by administration of the compositions.
WO2010131118A3 Polymorphs of etravirine and processes for preparation thereof The present invention provides novel crystalline forms of etravirine such as forms A, B, D, E, H, J, K, L and M, pharmaceutical compositions comprising the crystalline forms and method of using at least one of the crystalline forms or pharmaceutical compositions to treat HIV. Formula (I)
US20100168202 Rad 9 as a diagnostic,prognostic,and therapeutic tool for prostate cancer This disclosure provides a method of treating a human subject having a cancer which comprises administering to the subject a nucleic acid so as to inhibit expression of human RAD9 protein in a cell of the cancer so as to thereby treat the human subject. This disclosure also provides methods of assessing gains in prostate cancer therapy and detecting prostate cancer.
EP1390029B1 Phenylindoles for the treatment of hiv The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.
CN102731285A Anthraquinone compounds and applications thereof The invention relates to a class of anthraquinone compounds and applications thereof. The compounds have a structure represented by a general formula I, wherein R1 is selected from Br and XPH-(o, m, p)R3, X is O or S, R3 is selected from H, halogen, a saturated or unsaturated alkyl group containing carbon atoms of 1-6, an alkoxy group containing carbon atoms of 1-4, an amino group, and a phenyl group, and R2 is H or OH. The anthraquinone compounds of the present invention can be adopted as an analog of BH3-only protein, and can be competitively combined with proteins of Bcl-2, Bcl-XL and Mcl-1 or antagonize proteins of Bcl-2, Bcl-XL and Mcl-1, such that apoptosis is specifically induced while cell killing effects are not provided for normal cells and tumor cells missing Bax and Bak. The anthraquinone compounds of the present invention are expected to be developed into Bcl-2 family protein-targeting safe and efficient protein inhibitor drugs.
US20060106073 Process for the preparation of epothilone derivatives, new epothilone derivatives as well as new intermediate products for the process and the methods of preparing same The present invention provides a synthesis for the preparation of epothilone derivatives of formula 9 wherein R1 is methyl, and R2 is an unsubstituted or substituted aryl; an unsubstituted or substituted heteroaryl; or an unsubstituted or substituted heterocyclic radical fused to a benzene nucleus; and salts thereof, and intermediates for the synthesis of a compound of formula 9
US20080318912 Medicaments for Treating Chronic Respiratory Disease There is provided the use of a methylxanthine compound and a steroid in a synergistic combination for the treatment of a respiratory disease, wherein the methylxanthine compound is administered at a dose, which, in isolation, is not effective to treat said disease.
WO2013137479A1 Decahydroquinoxaline derivatives and analogs thereof A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents -O- or -CH2-; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
US20080039531 Compositions, and kits comprising targeted aldehyde or acetal protease inhibitor compounds for treating muscle disorders Described herein are compounds that comprise a carrier residue that is or is an analog of carnitine, an optional linker group, and a residue of a protease inhibitor comprising an aldehyde group or acetal derivatives of the aldehyde group, and pharmaceutical compositions and kits thereof. The compounds, compositions, and kits are useful for treating muscle disorders in animals and humans that result from the undesired activity of biological proteases. The compounds of the invention are particularly effective as calpain inhibitors, and can be used to treat the resulting muscular disorders, exemplified by Duchenne or Becker muscular dystrophy.
CA2696113A1 Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof Disclosed herein are tissue-nonspecific alkaline phosphatase (TNAP) activators and uses thereof for promoting bone mineral deposition.
CN1823751A Metoclopramide oral cavity disintegrating tablet and its production method An oral disintegrating tablet of metoclopramide as the dopamine acdeptor depressant is prepared from metoclopramide, cross-linked carboxymethyl cellulose sodium (CCNa) as disintegrant, and microcrystalline cellulose-90 (or 50) (CMCC-90 or 50) as diluent.
EP1330451B1 Substituted benzimidazol-2-ones as vasopressin receptor antagonists and neuropeptide y modulators The invention is directed to substituted benzimidazol-2-ones of Formula (I), wherein A, X, Y, m, n, R1, R2, R3, R4, and R5 are as described in the specification, which are useful as vasopressin receptor antagonists or Neuropeptide Y Modulators for treating conditions such as aggression, obsessive-compulsive disorders, hypertension, dysmenorrhea, congestive heart failure/cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, edema, ischemia, stroke, thrombosis, water retention, nephrotic syndrome, central nervous injuries, obesity, anorexia, hyperglycemia, diabetes, anxiety, depression, asthma, memory loss, sexual dysfunction, disorders of sleep and other circadian rhythms, and Cushing's disease.
EP1143976B1 Beta-d-2', 3' -didehydro-2', 3' -dideoxy-5-fluorocytidine for use in the treatment of hiv infections The present invention discloses a method for treating HIV that includes administering β-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using β-D-D4FC as 'salvage therapy' to patients which exhibit drug resistance to other anti-HIV agents. β-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.
US20110077285 Rna antagonist compounds for the modulation of pik3ca expression The invention relates to oligomeric compounds (oligomers), which target PIK3CA mRNA in a cell, leading to reduced expression of PIK3CA. Reduction of PIK3CA expression is beneficial for the treatment of certain medical disorders, such as hyperproliferative diseases (e.g., cancer). The invention provides therapeutic compositions that include the oligomers and methods for modulating the expression of PIK3CA using the oligomers, including methods of treatment.
CA2718209A1 (hetero)aryl cyclohexane derivatives The invention relates to compounds which have an affinity for the µ opioid receptor and the ORL1 receptor, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.
CN1165483B Compositions of ciplatin in comination with 2,2'-dithio-bis (ethanesulfonate) (dinesna) Co-administration of cisplatin with a pharmaceutically acceptable form of 2,2'-dithio-bis(ethanesulfonate) reduces the nephrotoxicity and myelosuppression of cisplatin and potentiates its anti-tumor action. Preferably the cisplatin and sulfonate are formulated as a composition, especially a sterile injectable solution containing chloride ions and sodium and hydrogen cations.
CN101817862A Ursolic acid-3-O-beta-D-pyranglucuronide and derivatives thereof, and preparation method and medicinal application thereof The invention discloses an ursolic acid-3-O-beta-D-pyranglucuronide and pharmaceutically acceptable salts or esters thereof, and a preparation method and a medicinal application of a compound, and especially an application in preparing medicaments for resisting diabetes and complications thereof. The ursolic acid-3-O-beta-D-pyranglucuronide and pharmaceutically acceptable salts or esters thereof have obvious function of reducing blood sugar, and especially have favorable efficacy of reducing hyperglycemia after meals.
WO2005121088A1 New disubstituted phenylpiperidines as modulators of dopamine and serotonin neurotransmission The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho,meta disubstituted phenyl)-1-alkypiperidines. (I) wherein R1, R2, and R3 are as defined.
CN103193695A 3-phenyl-3-pyrrolyl pentane derivative and medical application thereof The invention relates to the field of pharmaceutical chemistry, and in particular relates to a 3-phenyl-3-pyrrolyl pentane derivative (I) shown in the specification, wherein R1, R2, R3, R4 and R5 are defined in the specification. A pharmacodynamic experiment shows that the compound has effects of treating psoriasis and resisting tumor. The invention also discloses a preparation method of the compound.
WO2008047574A1 Sensitizer for anticancer agent It is clarified that the inhibition of the function or expression of 27 kinds of proteins, which participate in the repair and stabilization of chromosome, results in an effect of potentiating the anticancer effect of a known anticancer agent. Compound which inhibit the function of these 27 kinds of proteins or the expression of genes encoding these proteins are useful as a sensitizer for an anticancer agent. A medicinal composition comprising such a compound as described above makes it possible to reduce the dose of a therapeutic used in treating cancer. Also, this composition is usable as a drug to be combined with an anticancer agent which shows little side effects.
WO2013112673A1 Synthetic voacangine Synthetic voacangine, including in substantially enantiomerically enriched forms, and derivatives thereof are provided.
CN103271902A Slightly-soluble medicine solid dispersion and preparation method thereof The invention provides a slightly-soluble medicine solid dispersion and a preparation method thereof. The solid dispersion consists of a slightly-soluble medicine, liquid polyethylene glycol and a high-molecular carrier material, wherein the slightly-soluble medicine (polyphenolic hydroxyl medicine such as genistein and the like) is dissolved in the liquid polyethylene glycol (different from organic solvents); the liquid polyethylene glycol is used as a solvent as well as a plasticizer and can be completely dissolved with the high-molecular carrier material; the glass transition temperature is obviously reduced, the thermal decomposition of the slightly-soluble medicine and the high-molecular carrier material in a melting process is avoided, and solvent removal is not required; the solid dispersion is economical and nontoxic; the technology is simple, convenient and easy to implement, suitable for industrial production and favorable for popularizing a melting method to the preparation of an unstable medicine solid dispersion, and expands the selection range of the medicine and the carrier material; and in-vitro dissolving experiments prove that the solid dispersion provided by the invention can obviously improve the dissolution rate and solubility of the medicine.
US20130040921 Anticancer steroidal lactones unsaturated in position 7 (8) A compound of general formula (I), wherein R1-R17 and the ------ line take various meanings for use in the treatment of cancer.
CN102000219B Medicament for treating burns and scalds as well as preparation and use method thereof The invention discloses a medicament for treating burns and scalds as well as a preparation and use method thereof. The medicament is mainly prepared from root of monkshoodvine, borneol, peanut oil and poppy shells, wherein the preferential weight proportion relation of the root of monkshoodvine to the borneol to the peanut oil to the poppy shells is 10:1:12:0.6-1. The preparation method comprises the following steps of: firstly, preparing the root of monkshoodvine into dry powder; heating the peanut oil until the peanut oil smokes, and placing the poppy shells into the peanut oil, frying for 3-10 minutes, and de-slagging to obtain peanut oil filtering liquid; heating the peanut oil filtering liquid to boil; adding the borneol into the oil until the borneol becomes yellow; and finally adding the dry powder of the root of monkshoodvine into the peanut oil to prepare the materials into an external dosage form. In addition, the invention also discloses a combined medicament consisting of the medicament and garden burnet root dry powder agent. The medicament has the advantages of scientific and simple formulation, convenience in obtaining medicinal materials, all-around medicinal effect, simple preparation process, long storage time, convenience in use and the like, and is obvious in curative effect without leaving any scars, and the total effective rate and the healing rate areup to 100 percent.
US20110268791 Porous nanoparticle supported lipid bilayer nanostructures Various exemplary embodiments provide protocell nanostructures and methods for constructing and using the protocell nanostructures. In one embodiment, the protocell nanostructures can include a core-shell structure including a porous particle core surrounded by a shell of lipid bilayer(s). The protocell can be internalized in a bioactive cell. Various cargo components, for example, drugs, can be loaded in and released from the porous particle core of the protocell(s) and then delivered within the bioactive cell.
CA2268886C Aminothiophenecarboxamides Aminothiophene carboxylic acid amides having formula (I) and their physiologically harmless salts, wherein R1, R2, R3, R4, R5, A and n have the meaning given in claim 1, demonstrate phosphodiesterase V inhibition and can be used to treat cardiovascular diseases and in therapy for disturbances of potency.
US7847095 Process for 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1.,2,4-triazol-3-one The present invention is concerned with a novel process for the preparation of the compound 5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4 -tria-zol-3-one. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of psychiatric disorders, inflammatory diseases and emesis.
CN102488885A Marine organism bacteria-removing liquid for pet The invention relates to marine organism bacteria-removing liquid for a pet, which can be used for disinfecting a pet feeding environment, fur and wounds of the pet and pet supplies and deodoring the pet. The product can effectively kill pathogenic enterobacteria, pyogenic cocci and pathogenic yeast, has the bacteria-removing rate of 99.99 percent, can effectively prevent various infectious diseases, is an ideal disinfectant for a house pet, a pet shop and a zoo, is a marine organism environment-friendly product, does not contain harmful substances such as iodine, chlorine, aldehyde, phenol, mercury and the like, does not have any adverse effect on people and livestock, and is colorless, odorless, non-toxic, corrosion-free and non-irritant; and the production process is simple, cost price is low, and environment friendliness is achieved. The marine organism bacteria-removing liquid for the pet comprises the following components in percentage by weight: 6.0 to 7.0 percent of marine bios, 3.0 to 4.0 percent of cationic polymerization guanidine, 0.5 percent of bacitracin, and the balance of purified water.
CN101352429A Use of tiopronin in preparing medicament for treating liver function damage induced by cerebral ischemia, diabetes and obesity The invention relates to tiopronin or medical new use of the sodium salt thereof, in particular to the application of the tiopronin or the sodium salt thereof in the preparation of medicine for treating liver functional damage caused by cerebral ischemia, diabetes and obesity. The tiopronin has the function of specifically inhibiting liver cytochrome P450 2E1 (CYP2E1), there protecting the liver function from being damaged caused by cerebral ischemia, diabetes and obesity, so as to be a new clinical use having direction. The new use further expands the medical value of the tiopronin, which is taken as an inhibitor of liver CYP2E1 for protecting the function of liver, thus having important medical value, social and economic benefits.
US6989381 Containing s cyclodextrin compound in a concentration sufficient to maintain the drug in solution at such a drug concentration. There is provided a pharmaceutical composition for therapeutic or prophylactic administration to a subject having an infective disease or condition or at risk thereof. The composition comprises an aqueous carrier having in solution therein (a) an oxazolidinone antimicrobial drug, for example linezolid, in a therapeutically or prophylactically effective drug concentration that is above the practical limit of solubility of the drug in a substantially isotonic aqueous solution at a physiologically compatible pH, and (b) a pharmaceutically acceptable cyclodextrin compound in a concentration sufficient to maintain the drug in solution at such a drug concentration. The composition is particularly useful for intravenous delivery of the drug.
CN101647795B Application of Xyloketal B in preparation of medicine for treating radical damage disease The invention discloses application of xyloketal B in preparation of medicine for treating radical damage disease. The compound can directly eliminate the activity of radical, can obviously reduce radical peroxidation damage and has obvious protection effect on ischemia anoxia damage of nerve cell. The application of xyloketal B in preparation of medicine for treating radical damage disease in the invention excavates new medical usage of xyloketal B and opens up a new application field, and xyloketal B is safe and non-toxic, has strong pharmacological action and has good medical prospect.
WO2013002313A1 Weight control drug It was found that a compound represented by formula (I) has an LDL cholesterol reducing action, a blood pressure lowering action, a liver function improving action, and a uric acid level reducing action. A pharmaceutical composition comprising the compound is useful for weight control of a patient with obesity.
WO2005027934A1 Prolyl oligopeptidase inhibitor A prolyl oligopeptidase inhibitor which contains as an active ingredient either an α-acylamino-N-(diaminophosphinyl)lactam derivative which is a compound represented by the general formula (1) [wherein Q represents -(CH2)n- (n is 0 to 3); R represents hydrogen, alkyl, aryl, etc.; X represents carbonyl, etc.; and Y and Z each represents hydrogen, sulfo, acyl, alkyl, aryl, etc.] or a pharmacologically acceptable salt thereof.
CN102719521A Application of cystine/glutamic acid reverse transporter xCT inhibitor in treating liver cancer The invention provides an application of a cystine/glutamic acid reverse transporter xCT inhibitor in treating liver cancer, particularly provides a highly expressed marker xCT in live cancer. In addition, the expression or activity of the xCT is related to prognosis of patients, thus the expression of the xCT in liver cancer cells or tissues can be used for auxiliarily diagnosing or determining the probability of cancer occurrence in subjects and used for prognosis of liver cancer patients. The invention further provides a corresponding detection method, a kit and a screening method.
EP1832586A1 Thiazole-piperidine derivatives in treatment of diseases of liver and the pancreas The present invention relates to the use of piperidinyl-thiazole derivatives of formula (1) in the treatment and prevention of diseases of liver and the pancreas, wherein the substituents have the meanings explained in the description, and to particular compounds suitable for this use and to pharmaceutical compositions containing them.
US20090227665 Methods and Compositions For The Prevention and Treatment of Kidney Disease The invention provides compositions for preventing or treating kidney disease and improving kidney function comprising at least two ingredients selected from the group consisting of antioxidants and mitochondrial cofactors in amounts sufficient for preventing or treating kidney disease or for improving kidney function and methods for preventing and treating kidney disease or improving kidney function comprising administering such compositions to an animal susceptible to or suffering from kidney disease or impaired kidney function. In a preferred embodiment, the composition is admixed with one or more food ingredients to produce a food composition useful for preventing or treating kidney disease and improving kidney function, particularly in senior animals.
US7378397 Peptide derivatives; thyrotropin-releasing hormone-degrading; brain and spinal injuries, central nervous system disorders Peptide derivatives useful as inhibitors of activity of thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) are of formula Ia: wherein: R1 is an optionally substituted 4-, 5- or 6-membered heterocyclic ring having one or more heteroatoms, in which at least one carbon atom of the ring is substituted with O or S; X1 is —CO— or —CS— or —CH2CO— or CH(R4) wherein R4 is H or optionally substituted alkyl or —COOH or —COOR11 wherein R11 is optionally substituted alkyl; X2 and X3 (which may be the same or different) are —CO— or —CS—; Z is —CH2— or —S— or —O— or —NH—; Q is O or S; R2 is H or optionally substituted alkyl or an optionally substituted carbocyclic ring; R3 is H or optionally substituted alkyl or an optionally substituted mono- or polycyclic ring, optionally having one or more heteroatoms in the ring(s) and optionally being a fused ring; or R2 and R3 together form an optionally substituted mono- or polycyclic ring optionally having one or more heteroatoms in the ring(s) and optionally being a fused ring; R5 and R6 (which may be the same or different) are H, or lower alkyl; R7 and R8 (which may be the same or different) are H, or optionally substituted lower alkyl; R9 and R10 (which may be the same or different) are H, or optionally substituted alkyl, or an optionally substituted carbocyclic ring; Y is —(CH2)n— where n is 0, 1, 2 or 3 provided that when R2 and R3 form part of the ring n is 0; and pharmaceutically acceptable salts thereof.
US20100179208 Use of HDAC Inhibitors for the Treatment of Bone Destruction The present invention relates to the use of HDAC inhibitors for the treatment of bone destruction caused by cancer, inflammatory diseases and osteoporosis.
US20090130232 Composition and method for treatment of oral inflammation an ulceration The present invention is a composition and method for treating oral lesions. A composition for treatment of oral lesions may comprise: (a) an anesthetic composition; (b) an antifungal composition; (c) a steroid composition; (d) an antihistamine composition; and (e) an antacid composition, wherein the therapeutic composition is substantially free of alcohol. A method for treatment may comprise: (a) administering to a patient an effective amount of a composition, the therapeutic composition comprising: (i) an anesthetic composition; (ii) an antifungal composition; (iii) a steroid composition; (iv) an antihistamine composition; and (v) an antacid composition, wherein the therapeutic composition is substantially free of alcohol. A method of producing a composition may comprise: combining (a) an anesthetic composition, (b) an antifungal composition, (c) a steroid composition, (d) an antihistamine composition, and (e) an antacid composition, wherein the therapeutic composition is substantially free of alcohol.
US20120294831 Use of thiazolide compounds for the prevention and treatment of viral diseases, cancer and diseases caused by intracellular infections The invention provides for the use of pharmaceutical compositions comprising a thiazolide in the stimulation of the immune system in a subject in need thereof, thereby preventing and/or treating viral diseases, cancer and diseases caused by intracellular protozoan infections
CN1742734A Cefadole oral liquor antibacterial composition The present invention discloses an oral antimicrobial medicine composite composed of cefaclor and sulbactam pivoxil. The weight ratio range of cefaclor and sulbactam pivoxil in said oral antimicrobial medicine composite is 1:1 to 15:1, and the optimized weight ratio range is 1:1 to 6:1.
WO2009088042A1 Atomizing agent for prevention of infection with influenza virus Disclosed is an atomizing agent for preventing the infection with an influenza virus. Specifically disclosed is an atomizing agent for preventing the infection with an influenza virus, which comprises an aqueous solution or an alcohol solution having an alcohol content of 10 to 60%, wherein the aqueous solution or the alcohol solution contains hinokitiol, a metal complex thereof, or a salt of hinokitiol or the metal complex.
CN101756995A Application of 11, 28-dihydroxy-oleanane-2, 12-diene in preparing medicine treating skin diseases The invention relates to application of 11, 28-dihydroxy-oleanane-2, 12-diene in preparing a medicine treating skin diseases and provides a medicine composition. The medicine composition is characterized by containing the 11, 28-dihydroxy-oleanane-2, 12-diene (I) used as an active component and one or more medicinally auxiliary materials. In the medicine composition, the medicinally auxiliary materials are all auxiliary materials suitable for skin or mucosa administration.
WO2006035277A2 Novel processes for preparing amorphous rosuvastatin calcium and a novel polymorphic form of rosuvastatin sodium Provided are processes for preparing amorphous rosuvastatin calcium from crystalline rosuvastatin calcium by simple precipitation processes. Also provided is a novel polymorphic form of rosuvastatin sodium, processes for preparing thereof and pharmaceutical compositions thereof.
US20080004233 Delta-Tocotrienol Treatment and Prevention of Pancreatic Cancer Methods are disclosed for treating neoplastic disorders, such as pancreatic cancer, using tocotrienols; namely, gamma-tocotrienol and delta tocotrienol. The antitumorogenic effects of these compounds are shown both in vitro and in vivo using several human pancreatic cancer cell lines and MIA-PACA2 human pancreatic cancer cells xenografted in nude mice. Also disclosed are methods of testing the efficacy of potential chemotherapeutic agents by measuring their effect on surrogate endpoint biomarkers, such as Ki-67 and p27. Associated compounds are also disclosed.
WO2014015175A1 Compositions and methods for modulating brd4 bioactivity Compositions and methods for increasing or decreasing DNA repair are provided. Composition includes a Brd4 polypeptide, fragment, fusion, or variant thereof. The fusion protein can include a protein transduction, a targeting domain, or a combination thereof to enhance delivery of the fusion protein to the interior of a particular target cell, such as a cancer cell. Inhibitory nucleic acids that target a Brd4 mRNA and antibodies that target a Brd4 polypeptide are also disclosed. The inhibitory nucleic acid or antibody can target a sequence or epitope on Brd4 isoform B that is absent on Brd4 isoform A and Brd4 isoform C. Methods for increasing or decreasing the sensitivity of cells to a DNA damaging agent, methods of treating cancer, and methods of determining cells' sensitivity to a DNA damaging agent are also disclosed.
CN101933927A Composition containing enrofloxacin hexahydrate and application thereof to preparation of medicaments for treating or preventing diseases of domestic animals The invention relates to a composition containing enrofloxacin hexahydrate and application thereof to the preparation of medicaments for treating or preventing diseases of domestic animals and mycoplasma infection diseases. The composition has the characteristics of high in-vivo plasma peak concentration of the domestic animals, high bioavailability, and pharmacokinetics and clinical effect superior to those of enrofloxacin composition medicaments, can replace enrofloxacin and a composition thereof, is applied to the preparation of veterinary medicaments which are used clinically and widely, and has the wide market prospect and high value.
EP1669067A2 Flavonoids for cystic fibrosis therapy Compositions and methods for therapy of cystic fibrosis and other conditions are provided. The compositions comprise one or more compounds such as flavones and/or isoflavones capable of stimulating chloride transport in epithelial tissues. Therapeutic methods involve the administration (e.g., orally or via inhalation) of such compositions to a patient afflicted with cystic fibrosis and/or another condition responsive to stimulation of chloride transport.
CN102772729A Medicament for treating nasitis and preparation method thereof The invention discloses a medicament for treating nasitis and a preparation method thereof. The medicament is prepared from astragalus mongholicus, sharpleaf galangal fruit, schisandra chinensis, hemlock parsley, cochinchnese asparagus root, Chinese angelica, white peony root and the like in a certain weight proportion. The medicament has the functions of diminishing inflammation, promoting the restoration of consciousness, warming the medium and strengthening body resistance, and eliminating pathogen, and has the advantages of quick response, good curative effect and no relapse in treating nasitis.
WO2013179910A1 Agent for preventing and/or treating peripheral neuropathic pain caused by anti-cancer drug A medicine effective in preventing and/or treating peripheral neuropathic pain, such as allodynia, caused by an anti-cancer drug treatment; wherein the medicine contains thrombomodulin as an active ingredient.
US8263584 Imidazopyridines The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.
WO2014154921A1 Method for the synthesis of homologous compounds of azanucleosides The invention relates to the method for the synthesis of homologous compounds of azanucleosides, to the compounds produced by said method, and to the use of same for developing drugs for treating viral and bacterial diseases and cancer.
WO2003057161A3 BENZOTHIENO [3,2-c]PYRAZOLYL AND BENZOFURANO [3,2-c] PYRAZOLYL COMPOUNDS, THEIR USE IN DISEASES ASSOCIATED WITH THE 5-HT2C RECEPTOR AND INTERMEDIATE COMPOUNDS THEREOF Disclosed are benzothieno[3,2-c]pyrazolyl and benzofurano[3,2-c]pyrazolyl compounds of the formula (I) and (II), and intermediates of the formula (Ia) and (IIa) which are tautomers, wherein the variables A, X, y, R1, R2, R3 and R4 are as defined in the specification. The compounds are useful for the treatment or prevention of diseases and/or behaviors involving the 5-HT2C receptor site.
EP2560966A2 Multisubstituted aromatic compounds as inhibitors of thrombin There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.
US6846811 For treating psoriasis, inflammation, leukemia, colon cancer, breast cancer or prostate cancer This invention discloses (20S)-1α-hydroxy-2α-methyl-19-nor-vitamin D3 and (20S)-1α-hydroxy-25-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anticancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
US7445801 Stable bicarbonate-based solution in a single container Stable single bicarbonate-based solutions are provided. The bicarbonate-based single solution of the present invention includes at least calcium and bicarbonate and is stored or packaged in a sterile manner within a container with a gas barrier. The single solutions of the present invention can remain stable for three months or more. In this regard, the stable and single bicarbonate-based solutions of the present invention can be readily and effectively used during medical therapy, such as dialysis therapy.
CN102309667A Ointment for treating scald and preparation method thereof The invention discloses an ointment for treating scald, and the effective ingredients comprise the following components: aloe, pumpkin, peanut oil, egg white, mint, borneol, eucalyptus oil, panax notoginseng, dragon blood, ossa draconis, Chinese prickly ash, and salt. The ointment of the invention is used to treat scald, has a high cure rate and good curative effect. The preparation method disclosed by the invention comprises the following steps: weighing above raw material components which are prepared into effective ingredients on a weight basis; extracting the effective ingredients of aloe and pumpkin by microwave extraction technology, concentrating and drying the effective ingredients to obtain dry powder; roasting panax notoginseng and Chinese prickly ash with fire to become yellow, grinding panax notoginseng and Chinese prickly ash with dragon blood, ossa draconis, and borneol into powder, well mixing the prepared dry powder of effective ingredients of each components with peanut oil, egg white, and eucalyptus oil, performing high-temperature sterilization treatment to obtain the ointment for treating scald of the invention. The preparation method of the invention has simple steps, is easy to conduct, and has a stable process.
WO2013157984A1 preparation and method for the prophylaxis and treatment of osteoporosis and bone fractures A method for the prophylaxis and treatment of osteoporosis and bone fractures and a preparation for the prophylaxis and treatment of osteoporosis and bone fractures relate to medicine, in particular to means for preventive action in the event of conditions associated with various forms of osteoporosis. The method is characterized by a dose of from 10 mg to 1000 mg per day of drone brood and a vitamin or vitamins of group D, and/or active metabolites thereof of from 50 ME to 1000 000 ME per day, and a calcium compound of from 25 mg to 3000 mg per day, with simultaneous administration to an organism within a 24-hour period, where the preparation, consisting of from 10 mg to 1000 mg of drone brood, vitamin or vitamins of group D, and/or active metabolites thereof of from 50 ME to 1000 000 ME, and a calcium compound of from 25 mg to 3000 mg, can be realized in powdery, tablet or capsule form. Implementation of the invention provides for the achievement of the technical result which is envisaged by the applicant, which makes it possible to eliminate or reduce imbalance in the mineralization of various sections of bone tissue. The use of the claimed agent boosts the mechanism for uniformly restoring the mineral density of the bones, and the use of drone brood together with vitamin D is directed towards additional boosting of the remodelling of diseased sections of bone tissue and towards retaining bone tissue by maintaining the androgen level.
US20110288146 Directly compressible granular microcrystalline cellulose based, excipient, manufacturing process and use thereof An improved excipient comprising substantially homogeneous particles of a compressible, high functionality granular microcrystalline cellulose based excipient is provided. The improved excipient comprises microcrystalline cellulose and a binder, and optionally a disintegrant, and is formed by spraying a homogeneous slurry of the components. The excipient provides enhanced flowability/good flow properties, excellent/high compactibility, and increased API loading and blendability as compared to the individual components, and as compared to conventional excipients formed from the same materials. The improved excipient has strong intraparticle bonding bridges between the components, resulting in a unique structural morphology including significant open structures or hollow pores. The presence of these pores provides a surface roughness that is the ideal environment for improved blending with an API.
WO2007129169A3 Cox- ii inhibitors for improving reproductive success in a female animal Inhibitors of COX-II are useful for improving reproductive success in female animals.
WO2004105731A8 Nasal formulations including a topical decongestant and a topical corticosteroid and their use in treatment of obstructive sleep apnea A pharmaceutical formulation is provided for nasal drug administration of a topically administrable decongestant, a topically administrable corticosteroid and a pharmaceutically acceptable carrier, and may optionally include further carriers, therapeutic extenders, and the like. Such formulations may also optionally further include a therapeutically active member selected from the group consisting of a topical antibiotic, a topical antihistamine (preferably a non-sedating antihistamine), a leukotriene D4 antagonist, a 5-lipoxygenase inhibitor, and a FLAP antagonist, or a pharmaceutically acceptable salt thereof. In addition, methods for using the formulation to treat decongestant/corticosteroids-responsive conditions, diseases or disorders such as chronic obstructive nasal congestion and/or obstructive sleep apnea conditions, are provided, as are drugs delivery devices and dosage forms for housing and/or dispensing the formulations.
CN101982168B Quercetin nano-micelle preparation and preparation method thereof The invention discloses a quercetin nano-micelle preparation which is made from the following components in parts by weight: 20-40 parts of quercetin as a bulk drug and 220-330 parts of a pluronic surfactant as a drug carrier. A preparation method comprises the following steps: mixing the quercetin with the pluronic surfactant and dissolving in an organic solvent until being fully dissolved, and carrying out rotary evaporation at 15-60 DEG C for removing the organic solvent to obtain a drug-containing film; and drying the film in vacuum, adding a water phase for hydrating at 15-60 DEG C to obtain micelle solution, and filtering with a millipore filter to obtain the quercetin nano-micelle preparation. The obtained nano-micelle preparation has small nano-grade particle size of 20-60nm, a hydrophobic core and a hydrophilic shell, thus ensuring that the preparation has small possibility of being swallowed by a reticuloendothelial system in body, achieving effects such as targeting, long circulating and the like, and being beneficial to clinical application.
US8637087 Treatment of interstitial cystitis using (6aR, 10aR)-Δ8-tetrahydrocannabinol-11-OIC acids The present invention relates to non-psychoactive derivatives of tetrahydrocannabinol, which are useful in treating interstitial cystitis and relieving symptoms thereof. The invention uses (6aR,10aR)-Δ8-tetrahydrocannabinol-11-oic acids (hereinafter referred to as (6aR,10aR)-Δ8-THC-11-oic acid), as well as pharmaceutical compositions containing the (6aR,10aR)-Δ8-THC-11-oic acids, for treatment of interstitial cystitis in a mammal. The invention further covers methods of formulating and administering the compounds and pharmaceutical compositions as therapeutic agents in the treatment of interstitial cystitis, with particularly preferred administration routes being oral and via intravesicular instillation.
WO2010134091A1 A process for preparation of a non-antibiotic growth promoter formula / product and its use in food animals A Non-antibiotic growth promoter product as feed additive comprised of stabilized organosulfur compound(s) with or without flavor in the food animals for growth promotion, wherein in the organosulfur compounds is from the class of compounds of formula R- (S)n -R1 and the process for the preparation of the same.
US6893844 DNA encoding a new human hepatoma derived growth factor and producing method thereof The invention provides a cDNA sequence of a new type II human hepatoma derived growth factor (HDGF2). The protein encoded by such sequence is a homology of type I HDGF. The present invention also relates to peptides encoded by the nucleotide sequences, to uses of these polynucleotide and the polypeptides, and methods for producing the polynucleotides and the polypeptides.
US20120020977 Pancreatic cancer genes The present invention provides the art with the DNA coding sequences of polynucleotides that are up-or-down-regulated in cancer and dysplasia. These polynucleotides and encoded proteins or polypeptides can be used in the diagnosis or identification of cancer and dysplasia. Inhibitors of the up-regulated polynucleotides and proteins can decrease the abnormality of cancer and dysplasia. Enhancing the expression of down-regulated polynucleotides or introducing down-regulated proteins to cells can decrease the growth and/or abnormal characteristics of cancer and dysplasia.
CN102861002A Application and determining method of zinc ion as alpha-glucosidase inhibitor The invention relates to an application and a determining method of zinc ion as alpha-glucosidase inhibitor. The determining method includes the steps of firstly, preparing 0.6mM (mmol/L) zinc acetate, using 50mM ethanesulfonic acid (pH 6.5) buffer solution to dilute into different concentrations, and using 50mM phosphate buffer solution (pH 7.4) to prepare alpha-glucosidase into 3muMalpha-glucosidase liquid; secondly, mixing 30 microliters of zinc acetate of different concentrations with 30 microliters of alpha-glucosidase liquid, setting mixture of 30 microliters of buffer solution without zinc acetate and 30 microliters of alpha-glucosidase as blank control, preserving heat at 25 DEG C for 3 hours, and determining enzyme activity. Zinc ion has strong inhibition effect to alpha-glucosidase, and zinc ion can be used as effective substance for treating type-2 diabetes mellitus.
US20090054720 Use of histone deacetylase inhibitors in combination with radiation for the treatment of cancer The present invention relates to a method for the treatment of cancer in a patient in need thereof. The method comprises administering to a patient in need thereof a first amount of a histone deacetylase inhibitor in a first treatment procedure, and a second amount or dose of radiation in a second treatment procedure. The first and second treatments together comprise a therapeutically effective amount. The combination of the HDAC inhibitor and radiation therapy is therapeutically synergistic.
WO2010057118A2 Heterocyclic antagonists of prostaglandin d2 receptors Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
CN101854922A Drug depots having different release profiles for reducing, preventing or treating pain and inflammation Effective treatments of pain and/or inflammation are provided. Through the administration of an effective amount of at least analgesic and/or at least one anti-inflammatory agent at or near a target site, one can reduce, prevent or treat inflammation and pain.
US8716486 2-heterocyclylaminoalkyl-(p-quinone) derivatives for treatment of oxidative stress diseases Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.
WO2005009459A1 Ophthalmic compositions comprising trefoil factor family peptides This invention relates to compositions comprising trefoil family factor peptides which are useful in preventing or treating dry eye by topical administration of the composition to eye of the patient. One aspect of this invention relates to topical ophthalmic compositions comprising a trefoil factor family peptide, and preferably, a mucoadhesive component, as described herein. Another aspect of this invention relates to the use of these compositions to treat or prevent dry eye in a patient.
EP2558069A1 Benzonapthyridine compositions and uses thereof The present invention generally relates to compositions comprising benzonapthyridine small molecule immune potentiators (SMIPs) that are capable of stimulating or modulating an immune response in a subject that has had pre- or post-exposure to a pathogen such as hemorrhagic fever virus. Also provided are methods of preparing and using the SMIP compositions of the invention.
EP1173205B1 An oral formulation for ileum administering comprising an inhibitor compound of the ileal bile acid transport An oral pharmaceutical formulation comprising an inhibitor compound of the ileal bile acid transport (IBAT inhibitor compound) and a therapeutically acceptable carrier characterised in that the formulation is designed to deliver the IBAT inhibitor compound in the ileum. The IBAT inhibitor compound can also be administered in combination with a bile acid binder to alleviate possible side effects of therapy with IBAT inhibitor compound, such as for instance diarrhoea. The bile acid binder may be formulated for colon release.
US6887869 Mikanolide derivatives, their preparation and therapeutic uses The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents. The compounds correspond to general formula (1) corresponding to general sub-formulae (I)1 and (I)2, wherein: R1 represents H, SR4 or NR4R5; R2 represents SR6 or NR6R7; R3 represents OH, O(CO)R14, OSiR15R16R17, O(CO)OR18 or O(CO)NHR18, each of the radicals R4, R6, R15, R16 and R17 representing independently (in particular) an alkyl radical, the radicals R5 and R7 representing (in particular) radicals selected independently among a hydrogen atom and an alkyl radical, and each of the radicals R14 and R18 representing independently (in particular) an alkyl or cycloalkyl radical, or one among aryl, heteroaryl, aralkyl or heteroalkyl radicals optionally substituted; provided that when the compounds correspond to the general sub-formula (I)2, then R1 does not represent a hydrogen atom
CA2320039C Pharmaceutical composition comprising a combination of metformin and fibrate, and its use for the preparation of medicines intended to reduce hyperglycaemia The present invention relates to a pharmaceutical composition comprising, as active principles, (i) metformin optionally in the form of one of its pharmaceutically acceptable salts, and (ii) a fibrate chosen from fenofibrate and bezafibrate, in combination with one or more pharmaceutically acceptable excipients. These compositions are particularly suitable for the treatment of non-insulin-dependent diabetes.
CA2400312C Nutritional intervention composition for enhancing and extending satiety This invention relates to a nutritional intervention composition in a dry power form for enhancing satiety prior to a meal and extending satiety after a meal in a calorically efficient fashion. The dry nutrional composition includes protein, casein--macropeptide or glycomacropeptide, long chain fatty acids, soluble and/or insoluble fibers. The dry nutritional composition includes protein in the range of 0.22% to 88.30%, glycomacropeptide in the range of 0.06% to 87.72%, oleic acid in the range of 2.42% to 97.25%, soluble fibers in the range of 0.20% to 79.05%, and insoluble fibers in the range of 0.20% to 79.05%. The composition may also include plant saponins, calcium and cholestyramine.
WO2008060764A2 Topical therapies for oral mucositis and other conditions A method for treating oral mucositis in a subject comprises topically administering to an oral mucosal surface of the subject phenytoin or a pharmaceutically acceptable salt thereof in an amount effective to inhibit mucosal degeneration or promote mucosal regeneration, and optionally an analgesic agent in an amount effective, in combination with the phenytoin or salt thereof, to reduce pain associated with the oral mucositis. The phenytoin or salt thereof and optionally the analgesic agent can be administered in a pharmaceutical composition comprising an excipient vehicle suitable for intraoral administration, said composition being bioadhesive to an oral mucosal surface, for example having at least one non-lipoidal internal phase and at least one lipoidal external phase that is bioadhesive to said surface.
WO2012088597A1 Nitric oxide amino acid esters for enhancement of physical or muscular performance and the treatment of muscular or neuromuscular diseases Use of nitric oxide amino acid esters to treat muscular or neuromuscular diseases, increase muscle growth and/or muscle strength, or to stimulate vasodilation prior to physical training. Preferred muscular or neuromuscular diseases are muscular dystrophy and muscular atrophy. Preferably the nitric oxide acid esters are administered in a transdermal composition further comprising a penetration enhancer and a pharmaceutically acceptable carrier.
US7531175 Methods for modulation of immune responses using humanized immunoglobulins reactive with B7-1 molecules The invention relates to humanized anti-B7-2 and anti-B7-1 antibodies, wherein each comprise a variable region of non-human origin and at least a portion of an immunoglobulin of human origin. The invention also pertains to methods of treatment for various autoimmune diseases, transplant rejection, inflammatory disorders and infectious diseases by administering humanized anti-B7-2 and/or anti-B7-1 antibodies.
CN101724049A Human epididymal expression sperm binding protein HEL-207 as well as encoding gene and application thereof The invention belongs to the biotechnology and the medical field and discloses a new human epididymal specific expression sperm binding protein HEL-207 as well as preparation and application thereof. The invention discloses an amino acid sequence of the HEL-207 protein and provides a recombinant expression vector which carries a DNA sequence used for encoding the protein. The protein is located at the back part of the head of a mature sperm, an RT-PCR result indicates that the gene has expression in an epididymis tissue, a testis tissue, a cardiac tissue, a lung tissue, a liver tissue and a spleen tissue, and a band of about 46 KD is detected in an epididymis by using Western blot. The HEL-207 protein can be used as a target protein for developing an immunological contraceptive and clinically diagnosing and treating male infertility. A method for detecting a corresponding gene or protein based on development of the HEL-207 protein can be widely used for the research field of reproductive medicine.
US20120322788 Compouds The present invention relates to spirocyclic amide derivatives of the formula I, pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing them, and their use in therapy.
WO2011097594A3 Therapeutic methods and compositions involving allosteric kinase inhibition The present invention is directed to methods and compositions for suppressing lymphangiogenesis, angiogenesis and/or tumor growth. The methods comprise contacting the tumor with a compound that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state.
WO2013154303A1 Pyrimidine derivative substituted with novel hydrazine, and use thereof The present invention relates to a pyrimidine derivative substituted with novel hydrazine or a pharmaceutically acceptable salt thereof, and to a pharmaceutical composition for inhibiting c-Met tyrosine kinase activity and to a pharmaceutical composition for preventing or treating hyperproliferative disorders, which comprise same as an active ingredient. The present invention can be effectively used as a treatment agent for various hyperproliferative disorders related to excessive cell proliferation and growth caused by abnormal kinase activity, such as cancer, psoriasis, rheumatoid arthritis, and diabetic retinopathy by efficiently inhibiting c-Met tyrosine kinase activity.
CN102091075A Application of lipoxin for treating rheumatoid arthritis on the basis of inhibition action of lipoxin on multidrug resistance proteins The invention relates to application of lipoxin for treating rheumatoid arthritis on the basis of the inhibition of the lipoxin on multidrug resistance proteins. The subsidence of the synovium inflammation of a rheumatoid arthritis patient is promoted to treat the rheumatoid arthritis by replenishing the local lipoxin of joints on the basis of the inhibition action of the lipoxin on the multidrug resistance proteins. The invention overcomes the toxic side effect of the traditional drug and immune inhibition effect caused by closing cell factors. A method is simple, convenient and economic without inhibiting the immune functions of organisms, promotes the initiative subsidence of local inflammation and relieves the disease course development and the joint destruction; and in addition, the invention creates a new method for the treatment of the rheumatoid arthritis.
CN103611145A Medicament for treating simple struma and preparation method thereof The invention discloses a medicament for treating simple struma and a preparation method thereof. The medicament is mainly prepared from bryozoatum, leech and pangolin in a certain weight ratio. The medicament disclosed by the invention has the functions of depressing qi, warming the middle warmer, warming the kidney, absorbing qi, softening hard mass and treating stranguria, and has the advantages of quick response, good curative effect and no relapse of cured simple struma when being used for treating simple struma.
CN101675963A An externally-applied Zhengtong liquid An externally-applied Zhengtong liquid, relates to a Zhengtong liquid, in particular to a new type externally-applied Shuangzhui Zhengtong liquid, which is composed of 5 to 7 portions of trberculate speranskia herb, 3 to 5 portions of monkshood, 3 to 5 portions of cinnamomum cassia presl, 11 to 13 portions of borneol, 4 to 6 portions of rhizoma arisaematis, 4 to 6 portions of calcined marble, 3 to5 portions of borax, 4 to 6 portions of radix paeoniae rubrathe, and 3 to 5 portions of dahurian angelica root, which are immersed into alcohol for 40 to 50 days. The present invention not only can relieve pain, but also can promote blood circulation and remove blood stasis, eliminate inflammation and relieve pain, eliminate wind and disperse cold, and treat sprains.
CN101884631A Anti-tumor medicament based on alpha ketoglutaric acid and derivatives thereof The invention belongs to the technical field of biomedicine and relates to an anti-tumor medicament based on alpha ketoglutaric acid and derivatives thereof. The derivatives comprise various ester derivatives, amide derivatives and ether derivatives; and the alpha ketoglutaric acid comprises chemical analogues and derivatives thereof. The results of in-vitro experiments indicate that the mutation of isocitrate dehydrogenase in gliomas results in the loss of enzyme activities, the alpha ketoglutaric acid capable of growing in cells is obvious reduced, the levels of anaerobic inductor factors capable of inducing tumors and promoting the growth of the tumors are obviously improved, and the phenomenon can be reversed by exogenously replenishing absorbable alpha ketoglutaric acid. Therefore, an absorbable alpha ketoglutaric acid compound can be used for treating the gliomas, pancreatic cancers, breast cancers, liver cancers, lung cancers, gastric cancers, colorectal cancers, colon cancer and melanomas.
CN103725791A Egfr inhibitor treatment marker The present invention provides a biomarker that is predictive for the response to treatment with an EGFR inhibitor in cancer patients.
WO2013161823A1 Orally disintegrating tablet and method for producing same Provided are: an orally disintegrating tablet that disintegrates rapidly when held in the mouth or when placed in water, is palatable, possesses ample hardness for during normal production, transport, and use, and has excellent storage stability; and a method for producing the same with excellent industrial productivity. An orally disintegrating tablet, containing a drug, crystalline cellulose having a bulk density of 0.23 g/cm3 or less (preferably, 0.10-0.23 g/cm3), a sugar alcohol, and pregelatinized starch.
US20080153785 Pharmaceutical Compositions Containing Biophosphonate for Improving Oral Absorption Provided is a pharmaceutical composition having improved oral absorption of a bisphosphonate drug, comprising at least one active substance selected from bisphosphonate drugs having non-permeability to a lipid biomembrane due to ionization and high water-solubility in vivo and having bioavailability of less than 10%, and at least one selected from biocompatible water-soluble chitosan, as essential ingredients.
US20110251237 2,5-Disubstituted Piperidine Orexin Receptor Antagonists The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
CN102746181A 4-methoxy-N,N'-disubstituted phenyl-1,3-benzene diamide compounds and application thereof The invention aims at providing new 4-methoxy-N,N'-disubstituted phenyl-1,3-benzene diamide compounds which have anti-platelet-aggregation medical prospects, and application of the compounds in preparing anti-platelet-aggregation medicines. The 4-methoxy-N,N'-disubstituted phenyl-1,3-benzene diamide compounds provided in the invention are designed and produced on the basis of years of research results of the applicant, comprising eleven 4-methoxy-N,N'-disubstituted phenyl-1,3-benzenedicarboxamide compounds and four 4-methoxy-N,N'-disubstituted phenyl-1,3-benzenedisulfonamide compounds. Results of pharmacological tests in which external anti-platelet-aggregation activity is primarily screened show that the fifteen compounds of the invention have very high anti-platelet-aggregation activity, which is obviously higher than that of a positive contrasting medicine picotamide; and that the compounds of the invention has application prospect for being developed as new anti-platelet-aggregation medicines.
WO2009083155A1 Substance containing at least one active ingredient that has a gum-growing effect Disclosed is a substance which contains at least one active ingredient having a gum-growing effect and is used for treating gums in case of topical or general bone loss, especially for improving the phonetic and cosmetic situation of a patient and increasing cavity protection.
EP1501535A1 Antagonists of megalin or cubilin for use in preventing organ damage induced by therapeutic agents The invention relates to agents for the prevention of organ damage, in particular of the kidneys and the inner ear, induced by the administration of aminoglycosides. Agents according to the invention are all substances which are megalin and/or cubilin antagonists (inhibitors). In particular, these are molecules (compounds) having polybasic structures which bind to megalin and inhibit the binding of aminoglyco-sides and related substances.
US7138234 Gene involved in CADASIL, method of diagnosis and therapeutic application The invention concerns the Notch3 gene and the corresponding protein, which are involved in CADASIL. The invention concerns, in particular, methods for demonstrating mutations in this gene, which are linked to the risk of developing CADASIL and related diseases.
CN1965894B Prunella vulgaris polysaccharide having immune activity, preparation method and application thereof The invention relates to a prunella spike polysaccharide composite with immunity activity, and relative production, wherein its production comprises that: boiling the dry fruit of Prunella vulgaris L,extracting, depositing with alcohol, filtering the components whose molecule weight is higher than 3000Da, filtering and purifying. The polysaccharide content is higher than 50%, the polysaccharide molecule is higher than 5000Da. And it is formed by A, B-1, B-2, C, and D. The invention can improve lymphocyte transfer gain and induce IFN- gamma, to be used as active component to prepare the drug that improves the immunity of mammal.
US20070269524 Use of Idrocilamide for the Preparation of a Pharmaceutical Composition of Rosacea The invention relates to the use of idrocilamide for the preparation of novel pharmaceutical compositions, more particularly dermatological compositions, which can be used to treat rosacea.
CA2287907C Novel orally active iron (iii) chelators A novel 3-hydroxypyridin-4-one compound of formula (I) is provided, wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, R3 is selected from hydrogen and C1-6alkyl; and R4 is selected from hydrogen and C1-6alkyl, C1-6alkyl and a group as described for R2; characterised in that R2 is selected from groups (i) -CONH-R5, (ii) -CH2NHCO-R5, (iii) -SO2NH-R5, (iv) -CH2NHSO2-R5, (v) -CR6R6OR7, (viii) -CONHCOR5, wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-13alkyl, aryl and C7-13aralkyl, R6 is independently selected from hydrogen, C1-13alkyl, aryl and C7-13aralkyl, and R7 is selected from hydrogen, C1-13alkyl, aryl and C7-13aralkyl or a pharmaceutically acceptable salt of any such compound with the proviso that when R7 is hydrogen, R6 is not selected from aryl and with the proviso that the compound is not 1-ethyl-2-(1'-hydroxyethyl)-3-hydroxypyridin-4-one.
US7932276 administering a thiazole compounds with reduce side effect; 6-[2-(3,4-diethoxyphenyl)-thiazol-4-yl]pyridine-2-carboxylic acid The present invention provides a useful and highly safe agent for the treatment of chronic obstructive pulmonary disease, which contains, as the effective ingredient, at least one compound selected from the group consisting of thiazole derivatives and salts thereof represented by the general formula (1), wherein, R1 is a phenyl group which may have 1 to 3 lower alkoxy groups as the substituents on the phenyl ring; R2 is a pyridyl group which may have 1 to 3 carboxyl groups as the substituents on the pyridine ring.
WO2014086285A1 Antifungal compound and uses thereof Disclosed herein is a novel antifungal compound, derivatives that are used b treat fungal infections. In a specific embodiment, the compound is a small molecule. In a specific embodiment, the compound described herein inhibits yeast to hypha transition under robust hyphal inducing conditions at lower concentration of the molecule. Also disclosed is a composition comprising the antifungal compound. In a specific embodiment, the composition is a pharmaceutical composition Also disclosed is a method of treating and/or preventing fungal infection using the disclosed compound. The disclosed compound exhibits antifungal activity against wide range of fungal species at slightly higher concentrations. Antifungal compound disclose d herein is use d as anti-biofilm agent against fungal infections. In a specific embodiment, the disclosed compound is effective for systemic fungal infections. In a certain embodiment, the disclosed compound is a broad-spectrum antifungal agent for treating topical local and/or systemic fungal infections. In a specific embodiment, the disclosed compound is used in the prevention or treatment of mycotic infections caused by various fungal pathogens.
WO2010128663A1 Interleukin-2 production inhibitor A compound represented by one of formulae (I)-(V) or a pharmaceutically acceptable salt thereof is used as an active ingredient for an interleukin-2 production inhibitor. In formula (I), R1, R2 and R3 each represents a hydrogen atom or the same group selected from among alkyl groups having 1-5 carbon atoms, and X represents a halogen atom. In formula (II), R4 represents a hydrogen atom or an alkyl group having 1-5 carbon atoms, and X represents a halogen atom.
CA2824706A1 Pharmaceutical compositions for the treatment of parasitic diseases, cancer, or skin diseases by topical administration The present invention relates to pharmaceutical compositions for the treatment of parasitic diseases, cancer, or skin diseases by topical administration and especially ointments for the treatment of leishmaniasis. The present invention further relates to the use of the present ointments for the treatment of parasitic diseases, cancer, or skin diseases and especially ointments for the treatment of leishmaniasis in both humans and animals. Specifically, the present invention relates to pharmaceutical compositions such as ointments and cremes for the treatment of parasitic diseases, cancer, or skin diseases by topical administration comprising 0.1 to 20 weight%, preferably 0.1 to 10 weight%, more preferably 0.1 to 7 weight%, most preferably 0.5 to 5 weight%, of the pharmaceutical composition oleyl phosphocholine as an active ingredient.
US20110158935 Substituted Diketopiperazine Analogs for Use as Drug Delivery Agents Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.
US7459151 Phosphate-binding polymers for oral administration Phosphate-binding polymers are provided for removing phosphate from the gastrointestinal tract. The polymers are orally administered, and are useful for the treatment of hyperphosphatemia.
EP1633716A4 Biarylmethyl indolines, indoles and tetrahydroquinolines, useful as serine protease inhibitors The present invention provides compounds of Formula (I) or a stereoisomer or pharmaceutically acceptable salt or hydrate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4 and W are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
CN102688214A Preparation method of levetiracetam sustained release tablet The invention discloses a preparation method of a levetiracetam sustained release tablet, characterized in that an active ingredient, levetiracetam, is added in a prescription by several times, and plays roles of stable release, sustained release and quick release respectively; and moreover, a mixed retardant is prepared by adopting nanotechnology, and produced into the levetiracetam sustained release tablet. the levetiracetam sustained release tablet has the advantages that a release curve is close to an ideal release curve and a factor f2 is obviously superior to the factor f2 of products available in market, so that a satisfactory effect is obtained.
WO2014140644A1 Chemical entities Provided are chemical entities selected from compounds of formula (I), wherein R1, R2 and m have meanings given in the description, and pharmaceutically acceptable salts, solvates and stereoisomers thereof, which are inhibitors of ATR and are potentially useful in the treatment of cancer. Further provided are pharmaceutical compositions of the chemical entities, combination products containing the chemical entities, the use of the compositions as therapeutic agents, and methods of treatment using these compositions.
CN101721410A Solid medicinal composition of clopidogrel hydrogen sulfate The invention relates to an oral medicinal composition containing I crystal-form clopidogrel hydrogen sulfate, polyethylene glycol and micro-powder silica gel, proper disintegrating agent and filling agent. The auxiliary materials of the composition are low in price and can be obtained easily; the preparation process is simple; the requirement for equipment and environment is not high; and the prepared tablet is stable in quality and good in reproducibility, and is applied to industrialized production. The prepared tablet has good stability in long-term storage and can be maintained stable after being placed for 6 months at the temperature of 40 DEG C, without appearance change and obvious degradation or crystal-form inversion phenomenon; the dissolution rate of the tablet is not reduced after the tablet is placed for a long time; and the dissolution rate of the tablet in 10 minutes can still reach more than 95 percent after the tablet is placed for 6 months at the temperature of 40 DEG C.
US20120177735 Oral dosage formulation containing both immediate-release and sustained-release drugs for treating neurodegenerative disorders Disclosed herein is an oral dosage formulation that contains both immediate-release and sustained release drugs for treating neurodegenerative disorders. The immediate-release drug in the oral dosage formulation is an acetylcholinesterase inhibitor (AChEI) with a dissolution rate of releasing more than 80% of the AChEI within 60 min; and the sustained-release drug is memantine with a dissolution rate of releasing more than 80% of memantine within 12 hours.
CA2731498A1 Tri-cyclic pyrazolopyridine kinase inhibitors The present invention relates to compounds of the formula (I), which are useful as inhibitors of protein kinase The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the composi-tions in the treatment of various disease, conditions, or disorders The invention also provides processes for preparing compounds of the inventions
CN101932331A Methods for in vitro maturation of ovarian follicles The invention relates to methods to be used in the maturation of ovarian follicles and oocytes. More specifically, the invention concerns the use of inhibitors of the phosphatase PTEN, such as oxovanadate and peroxovanadate complexes, in methods for in vitro and in vivo maturation of follicles and oocytes.
WO2010132839A3 Aminoglycoside dosing regimens The present invention provides new aminoglycoside dosing regimens associated with enhanced microbicidal activity and reduced nephrotoxicity, as well as methods of using these dosing regimens to treat various bacterial infections.
EP1985297A1 Carboxylic acid compound and use thereof Provision of a superior URAT1 activity inhibitor effective for the treatment and the like of a pathology involving uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urinary lithiasis, renal dysfunction, coronary heart disease, ischemic cardiac diseases and the like. A URAT1 activity inhibitor containing a compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate thereof as an active ingredient: wherein each symbol is as defined in the specification.
US7166597 Antiinflammatory agents; autoimmune disease treatments; pyrazolo(1,5-a)pyridine derivatives Compounds of Formula (I): salts or solvates or physiologically functional derivatives thereof, wherein Z is CH or N, and R1, R2, and R4 are various substituent groups, are protein kinase inhibitors
US20120015027 F, G, H, I and K Crystal Forms of Imatinib Mesylate The invention relates to the F-crystal form, G-crystal form, H-crystal form, I-crystal form and K-crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, certain processes for their preparation, pharmaceutical compositions containing these crystal forms, their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans.
CN102008542A Compound neomycin sulfate soluble powder and production method thereof The invention provides compound neomycin sulfate soluble powder and a production method thereof. The soluble powder is prepared by mixing neomycin sulfate, doxycycline hydrochloride, trimethoprim, atropine sulfate, astragalus root extract, silicon dioxide fine powder and anhydrous dextrose. The obtained neomycin sulfate soluble powder is compounded by using multiple components, and has the effects of greatly reducing diarrhea of livestock and poultry animals, quickly recovering health status and the like.
DE102005015254A1 New indazole derivatives are serum and glucocorticoid regulated kinase inhibitors useful to treat and/or prevent e.g. diabetes, cardiovascular diseases, fibrosis and inflammatory diseases Indazole derivatives (I) and their tautomers, salts, solvates and/or stereo isomers are new. Indazole derivatives of formula (I) and their tautomers, salts, solvates and/or stereoisomers are new. R : H, A, COOA, CONHA, CONA2 or (CH2)mAr; B1>, B2>CH or N; R1>H, A, hal, CN, NO2, C(=O)A, CHO, CH(OH)A, NH2, NH(C=O)A, COOH, COOA, SO2NH2, CONH2, CONA2, (CH2)mAr or Het; R2>OH, OA, hal, CF3 or SO2NH2; R3H, hal, NH2, NHA, NA2, NHCOA, NHCONHA, NHCONHAr or Het1>; Ar : phenyl (optionally mono-, di-, or trisubstituted by hal, A, OH, OA, NH2, NO2, CN, COOH, COOA, CONH2, NHCOA, NHCONH2, NHSO2A, SO2NH2 and/or S(O)mA); Het : furyl, thienyl, pyrrolyl, imidazolyl, pyridyl, pyrimidinyl, pyrazolyl, thiazolyl or indolyl (mono-, di- or trisubstituted A, hal, OH and/or OA); Het1>morpholinyl, pyrrolidinyl, piperidinyl, pyrazolyl, furyl, thienyl, pyrrolyl, imidazolyl, pyridyl or pyrimidinyl (mono-, di- or tri substituted by A, hal, OH and/or OA); A : 1-10C alkyl (1-7 H optionally substituted F); X : CH2, CHA, CA2 or cycloalkyl compound of formula (Iz); hal : F, Cl, Br or I; m : 0-2; and n : 1-4. Independent claims are included for: (1) the preparation of (I); (2) a medicament comprising (I) and at least an active substance; and (3) a kit comprising (I) and other active substance in separate packings. [Image] [Image] - ACTIVITY : Antidiabetic; Nephrotropic; Neuroprotective; Dermatological; Anorectic; Analgesic; Antianginal; Cardiovascular-Gen.; Cardiant; Antiarteriosclerotic; Antiinflammatory; Hepatotropic; Antiarthritic; Antirheumatic; Nootropic; Cytostatic; Anticoagulant; Ophthalmological; Antibacterial; Tranquilizer. - MECHANISM OF ACTION : Serum and glucocorticoid regulated kinase inhibitor.
US20080051361 Intraocular pressure-related conditions, namely glaucoma; administering to the eye of the patient an interfering RNA molecule that attenuates expression of the GREM1 mRNA via RNA interference RNA interference is provided for inhibition of gremlin in intraocular pressure-related conditions, including ocular hypertension and glaucoma such as normal tension glaucoma and open angle glaucoma.
WO2008093678A1 Hyaluronidase inhibitor [PROBLEMS] To provide: a novel agent having an inhibitory activity on hyaluronidase; and an anti-aging agent for the skin, an anti-inflammatory agent and others each of which comprises the agent. [MEANS FOR SOLVING PROBLEMS] Disclosed is a hyaluronidase inhibitor comprising a phenylethanoid glucoside as an active ingredient. The phenylethanoid glucoside preferably comprises at least one of echinacoside and acteoside. Also disclosed is a hyaluronidase inhibitor comprising an extract of a plant belonging to the family Cistanche as an active ingredient. The extract of a plant belonging to the family Cistanche is preferably isan extract from a stem of a plant Cistanche tubulosa. Each of the hyaluronidase inhibitors can be used in a pharmaceutical product for a mammal including human, an external preparation for the skin, a food/beverage or a feed for a mammal as an active ingredient of an anti-aging agent for the skin or an anti-inflammatory agent.
US20130052156 Antiviral method This invention provides a method of inactivating non-enveloped virus particles. The method includes the step of contacting the virus with a virucidally-enhanced alcoholic composition that includes an alcohol, and enhancers selected from cationic oligomers and polymers, proton donors, chaotropic agents, and mixtures thereof.
WO2013059638A1 Combination treatment (eg. with abt-072 or abt -333) of daas for use in treating hcv The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1 (ABT) or therapeutic agent 2 (=ABT-333) or therapeutic agent 3 (=ABT-072) or therapeutic agent 4 (ABT), and an inhibitor of cytochrome P450 (e.g., ritonavir).
WO2014003541A1 Copper(ii) -mixed ligand complexes with anticancer properties The present invention discloses pharmaceutical composition having at least one of the series of ternary copper(II) complexes, [Cu(phen)(aa)(H2O)]ΝO3·xΗ2O from 1,10-phenanthroline and amino acid ligands. The said amino acid ligands are glycine (gly), sarcosine (sar), DL-alanine (DL-ala), or 2, 2-dimethylglycine (C-dMg). The series of ternary copper(II) complexes with anticancer properties are further characterized by selectivity towards cancer cells. The anticancer properties are due to increase reactive oxygen species (ROS) generation, selective induction of nuclear double strand DNA breaks (DSBs), cell cycle arrested at G0/G1, proteasome inhibition, oxidative DNA damage and topoisomerase I (topo I) inhibition.
EP2480545A1 Fused triazole amines as p2x7 modulators Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
CA2275379C Use of pramipexole in the treatment of restless legs syndrome The present invention provides the use of pramipexole in the treatment of restless legs syndrome.
EP1643965A2 Protection against sunburn and skin problems with orally-ingested high-dosage zeaxanthin A carotenoid substance called zeaxanthin, when ingested orally at suitable dosages such as 30 to 100 mg/day for a span of 1 to 2 weeks, can provide effective protection against sunburns, and can give skin a darker tint that emulates a healthy suntan. In tests involving adults, it was found that zeaxanthin dosages of 30 to about 80 mg per day were sufficient to induce: (i) a mild but noticeable tinting, shading, or darkening of skin color, comparable to a mild suntan; (ii) a substantial increase in the person's ability to withstand elevated levels of sun or UV exposure without any subsequent pain or discomfort, and without the subsequent peeling and flaking that characterizes sunburns; and, (iii) an increased ability of reddened and sunburned skin to convert into intact skin that looks browned and healthily tanned. By reducing the amount of exposure to sunlight (or tanning lights) that are required to achieve a desired level of tanning, zeaxanthin can reduce the risks of skin cancer, premature aging or wrinkling, and similar skin problems. Since zeaxanthin also has retina-protecting properties and reduces the risk of a disease called macular degeneration, oral ingestion of these dosages of a zeaxanthin to enhance a tanned appearance and/or to protect against sun damage is believed to pose no health risks, and can offer several benefits due to the anti-oxidant and other activities of zeaxanthin.
WO2010046445A2 Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use The present invention relates to compounds defined by formula I wherein the groups R1, Y1 to Y4, V, W, and X are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
CN103349711A Anti-aging combination with resveratrol and preparation method thereof The invention discloses an anti-aging combination with resveratrol and a preparation method thereof. The anti-aging combination with resveratrol is prepared with the following components by weight: 50 to 200 parts of resveratrol, 40 to 150 parts of acanthopanax senticosus extract, and 40 to 150 parts of wolfberry extract. The anti-aging combination with resveratrol prepared by the invention overcomes the defect that the action time of resveratrol in vivo is short when resveratrol is used alone, the addition of acanthopanax senticosus extractand wolfberry extract gives full play to synergistic effect between groups, the composition is good in stability and long in action time, the curative effect is improved, and the combination is provided with the functions of nourishing the kidney, strengthening the essence and boosting immunity, so as to delay senescence; the composition is safe and has no side effect.
DE202006003249U1 Preparation useful for treating wound, comprises natural complex of chitin, 1,3-beta-D-glucan, 1,6-beta-D-glucan and melanin that is produced from fungus of Fomes fomentarius, where component is used for powder basic substance Chitin, 1,3-beta-D-glucan, 1,6-beta-D-glucan and melanin wound powder comprising a natural complex of chitin, 1,3-beta-D-glucan, 1,6-beta-D-glucan and melanin, which is produced from a fungus of Fomes fomentarius, where the component is used for a powder basic substance or 100% of natural complex of the chitin-, 1,3-beta-D-glucan, 1,6-beta-D-glucan and melanin in strewing consistency, is new. - ACTIVITY : Vulnerary; Antibacterial; Fungicide; Virucide. No biological data given. - MECHANISM OF ACTION : None given.
CA2767833A1 N-acetyl cysteine compositions and methods to improve the therapeutic efficacy of acetaminophen The present invention relates to compositions for improving the efficacy of acetaminophen comprising a unit dose of acetaminophen and a therapeutic efficacy-enhancing amount of N- acetylcysteinc, such that acetaminophen and N-acctylcysteinc are present in the composition in a molar ratio of acetaminophen to N-acetyl cysteine ranging from about 1:15 to about 1:0.000977, and use of such compositions for analgesic and antipyretic applications.
CA2212207C Use of isoxazole and crotonamide derivatives for the modulation of apoptosis Compounds of the formula I or II (see formula I) (see formula II) are suitable for the production of pharmaceuticals for the modulation of apoptosis. These compounds can be employed for the treatment of infarct, stroke, neurodegeneration or hypertrophic disorders.
CN102309475A Levocarnitine for injection and preparation method thereof The invention discloses a levocarnitine for injection and a preparation method thereof. The preparation method comprises the following steps: weighing sodium dihydrogen phosphate and sodium hydroxide, using injection water to dissolve the weighed sodium dihydrogen phosphate and sodium hydroxide and diluting and uniformly mixing, dissolving levocarnitine and mannitol in the buffer solution, addingneedle active carbon and stirring uniformly, stirring for adsorption, and using filtering membrane for filtering and removing carbon; carrying out fine filtration through 0.22 mum microporous membrane, after the intermediate passed the inspection, filling the filtrate with the amount of 5 ml in 15 ml penicillin bottle (using up the liquor in 6 h after degerming), and carrying out half-plug pressing, freeze-drying, capping, visual inspection, labeling, and packaging. According to the invention, buffer salts (the buffer salt ion pair consisting of sodium dihydrogen phosphate and sodium hydroxide) with buffer effect are used in stead of traditional hydrochloric acid to regulate the pH value of the levocarnitine solution, so that the main drug is always in a stable pH environment in the wholepreparation process, and the API degradation caused by violent change of pH value of levocarnitine is avoided. Compared with the similar kind products, the levocarnitine disclosed in the invention has higher effectiveness and higher safety.
US20090082452 Deuterium-enriched lumiracoxib The present application describes deuterium-enriched lumiracoxib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20070293484 Thiophene Heteroaryl Amines The present invention relates to thiophene heteroaryl amines and their pharmaceutically acceptable salts that modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
CN102727518A Application of aluminum hydroxide compounds for preparing medicines capable of treating microbial persistent infection The invention belongs to the chemical medicine field, and relates to an application of aluminum hydroxide compounds for preparing medicines capable of treating microbial persistent infection. According to the invention, the aluminum hydroxide compounds can be taken as individual and unique component to perform normal mice and hepatitis B surface antigen transgene mice animal experiments, the result shows that the repetitive usage of aluminum hydroxide enables Grl<+> cell to enter into spleen and reduce the HBsAg level in mice serum; repetitious usage of aluminum hydroxide enables serum HBeAg of chronic hepatitis B patients to achieve transformation of mutating activity from positive to negative, and an antibody for anti-HBeAg is generated and the serum hepatitis B virus DNA is decreased. The individual and unique component aluminum hydroxide of the present invention can be taken as the novel medicine for treating chronic hepatitis B, can be subjected to further modification to increase the curative effect, or used for other persistent infection disease with other virus antigenemia, and combined with other medicines for experiments and clinical researches.
US20050070523 For therapy of bacterial infection in a mammal Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications, including using the invention compounds to treat bacterial infections.
US20120121531 Biocomposite for artificial tissue design The present invention concerns a biocomposite useful in artificial tissue replacement, methods for its production, and methods of use. The biocomposite can be implanted into humans or animals as an artificial tissue for treatment of a tissue defect. The biocomposite can be formed or manipulated into a desired shape for implantation.
CN101810606A Application of 2-(6-hydroxyl-2',3'-dimethoxyphenyl)-6-hydroxyl-7-methoxy benzofuran for preparing monoamine oxidase inhibitor The invention relates to a new application of 2-(6-hydroxyl-2',3'-dimethoxyphenyl)-6-hydroxyl-7-methoxy benzofuran, namely the application of the 2-(6-hydroxyl-2',3'-dimethoxyphenyl)-6-hydroxyl-7-methoxy benzofuran for preparing a monoamine oxidase inhibitor and a medicament for preventing and treating senile dementia.
US20070270442 Combination of a Cdk Inhibitor and Cs-682 or a Metabolite Thereof A first aspect of the invention relates to a combination comprising a CDK inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a CDK inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a CDK inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to a subject.
WO2014035295A1 Pharmaceutical composition for treating gastro-oesophageal reflux disease The invention relates to medicine and pharmacology, more particularly to drugs, and even more particularly to pharmaceutical compositions for treating gastro-oesophageal reflux disease (GORD). The pharmaceutical composition for treating GORD contains at least one proton pump inhibitor (PPI) and at least one prebiotic. Also claimed is a method for treating gastro-oesophageal reflux disease in which it is not necessary to eradicate the presence of H. pylori in order to prevent the risks associated with the translocation of said bacteria from the antrum to the body of the stomach. The composition provides for prevention of the translocation of H. pylori by means of the colonization of the antrum by lactobacilli and the concurrent inhibition of H. pylori during PPI therapy. This makes it possible to dispense with the need to detect the bacteria and carry out a course of eradication therapy. The safety of long-term PPI therapy is increased. Furthermore, the mucous membrane of the stomach does not undergo atrophy; consequently, there is no increase in the risk of stomach cancer.
WO2011025968A1 1h-pyrazolo [ 3, 4-b] pyridine compounds for inhibiting raf kinase Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. [FORMULA I]
EP1684765A1 Use of (2s, 3s) 2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol This invention relates to a novel use of (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol, in particular its use in the treatment of Restless Legs Syndrome, or its use in the treatment of Periodic Limb Movement Disorder (PLMD).
WO2007068212A1 Intravenous emulsion of butylbenzene phthalein and its application The present invention discloses an emulsion for intravenous injection or infusion, containing 0.01-50 wt.% butylbenzene phthalein or derivatives thereof as active ingredient, and 50-99.99 wt.% excipients, based on the total weight of emulsion.
CN103006799A Oral liquid clearing heat from throats and preparation method The invention discloses oral liquid clearing heat from throats and a preparation method. The preparation method comprises the following steps of: extracting medicine terminalia fruit with water, filtering the extract, concentrating the filtrate to obtain ointment 1, carrying out ethanol precipitation and recovering ethanol to obtain medicine terminalia fruit ointment; soaking indigo naturalis in a hydrochloric acid water solution, washing indigo naturalis until indigo naturalis is neutral and drying neutral indigo naturalis to obtain refined indigo naturalis; adding water to extract liquorice, filtering the extract, concentrating the filtrate to obtain ointment 2, adding ethanol to the ointment 2, standing, taking the supernatant, adjusting the pH value, filtering the supernatant, recovering ethanol from the filtrate, adding water, adjusting the pH value, filtering the solution, washing the precipitate with water and drying the precipitate to obtain a liquorice extract; and drying and grinding the medicine terminalia fruit ointment, mixing the medicine terminalia fruit ointment powder with ground refined indigo naturalis, calculus bovis factitius, borneol, menthol and the liquorice extract uniformly to obtain a mixture, adding distilled water with weight being 10-50 times that of the mixture and a flavouring agent with weight being 0.1-5 times that of the mixture and mixing the materials uniformly to prepare the oral liquid. The oral liquid is low in cost, is safe, takes effect quickly, has a good curative effect, is convenient to carry, costs few working hours, is high in active ingredient transfer rate and has high safety to operators.
US20080153817 Treatment for Alzheimer's Disease and Related Conditions Compounds of formula (I): are useful in the treatment of diseases associated with deposition of β-amyloid in the brain.
CN103238834A Composition for treating cutaneous pruritus and preparation method of composition The invention provides a composition for treating cutaneous pruritus. The composition comprises the following components in parts by weight: 3 to 10 parts of peach kernel extract, 4 to 15 parts of seville orange flower extract, 1 to 5 parts of folium mori extract, 1 to 6 parts of folia perillae acutae extract, and 3 to 10 parts of dark plum fruit extract. The composition harmonizes the blood, promotes the circulation of blood, expels the wind with diaphoresis, and inhibits the production of allergic factors in the body, aiming at allergic constitution in specific endowment constitution (represented by skin sensitivity), in order to reach the purposes of relieving skin allergy and cutaneous pruritus. Shown as the experimental results, the composition has the effects of resisting cutaneous pruritus and skin allergy.
US8247391 Macromolecules, lectins, dextrans, and/or concanavalin A moieties bind reversibly attached to crosslinked particles; sol-gel transformation; drug delivery The present invention relates to a gel composition, comprising first and second gel-forming moieties which bind reversibly to one another to form a gel. The binding of the moieties is sensitive to the level of an analyte, and either or both of the gel-forming moieties are attached to cross-linked particulate entities such that the interstices between the entities allow gel-sol and sol-gel transformation, and yet are not so small that the analyte cannot diffuse therethrough. The invention also provides drug delivery systems and sensors for detecting an analyte utilizing such a gel.
EP1709035A1 1 , 3 - dioxane derivatives and analogues thereof useful in the treatment of i.a. obesity and diabetes The present invention discloses novel compounds of formula (I) and their pharmaceutically useful compositions as modulators of PPAR ligands
WO2012160179A2 Topical pharmaceutical composition based on semifluorinated alkanes The invention provides liquid or semi-solid pharmaceutical compositions for topical administration comprising a semifluorinated alkane. The compositions are useful for the delivery of active ingredients into the deep layers of the skin or skin appendages. Various active ingredients may be incorporated, such as immunosuppressants, antiinfectives, antifungal agents, antiinflammatory agents, and retinoids.
EP2648722A1 Compositions for treating dermatitis and ichthyosis, and methods for treating dermatitis and ichthyosis A skin disorder treatment composition and method for treating a skin disorder or symptoms of a skin disorder are provided. The composition includes: about 0.0001 wt. % to about 5 wt. % of a serine protease inhibitor; about 2 wt. % to about 10 wt. % of a hydrophobic polymer/hydrophilic polymer complex comprising a poly(vinylpyrrolidone-alkylene) polymer wherein the alkylene group contains at least 10 carbon atoms and a cellulose containing polymer; about 0.5 wt. % to about 20 wt. % of a release agent; and at least about 50 wt. % water. The skin disorder or the symptom of skin disorder from ichthyosis, dermatitis, eczema, rosacea, psoriasis, inflammation, xerosis, or urticaria.
CN101474166B Cetirizine and pseudoephedrine sustained-release capsule and preparation method thereof The invention discloses a cetirizine pseudoephedrine slow release capsule. Cetirizine hydrochloride is prepared to quick release pellets and pseudoephedrine hydrochloride is prepared to slow release pellets, in accordance with the weight proportion that each 1000 preparations contain 5g of cetirizine hydrochloride and 120g of pseudoephedrine hydrochloride, the two pellets are uniformly mixed and encapsulated; or the two pellets are encapsulated respectively in proportion. The quick release part of the cetirizine hydrochloride and the slow release part of the pseudoephedrine hydrochloride are synthesized together subsequent to being prepared to the pellets respectively, so as to prepare the capsule with two different medicine-releasing speeds, the medicine-releasing speed of each pellet isuniform and the medicine effect is steady. The capsule has the advantages of even and extensive distribution of the medicine in vivo subsequent to the administering, sufficient absorption of the medicine, small stimulation to gastrointestinal tracts and good reproducibility of the medicine-releasing rule, and improves, while maintaining the properties of rapid effecting and long half-life of the cetirizine, the pharmacokinetic properties of the pseudoephedrine hydrochloride to administer twice per day instead of having to administer four times per day, so that both reach the optimal cooperative curative effect.
US20120328585 Nutritional Composition Having Prebiotic The present invention is directed to a novel method for increasing the production of acetate, decreasing the production of butyrate, increasing the population and species of beneficial bacteria and slowing the rate of fermentation of prebiotics within the gut of a formula-fed infant. The method comprises administration of a therapeutically effective amount of PDX to the infant.
US20120172283 Methods and compositions for targeted drug delivery Disclosed are Drug Delivery Molecules (DDMs) which both facilitate functional imaging, as by PET, MRI or SPECT, and create a biological effect and methods of their use. These DDMs which are variously designed to target specific receptors, internalized and then function biologically, as for purposes of cell destruction or therapy.
CN103462959A Application of Incarviatone A in medicaments for treating liver cancer The invention discloses an application of Incarviatone A in preparation of medicaments for treating liver cancer, and belongs to the technical field of a new application of medicaments. In-vitro methyl thiazolyl tetrazolium (MTT) anti-tumor activity evaluation discovers that the Incarviatone A has a prominent inhibiting effect on growth of human liver cancer cell strains HepG2, MHCC-LM3, Bel-7402 and HuH-7. Therefore, the Incarviatone A can be used for preparing anti-liver cancer medicaments, and has a good development and application prospect. The application of the Incarviatone A in preparation of the medicaments for treating the liver cancer is made public for the first time, the skeleton type is completely novel, and the Incarviatone A has an unexpectedly strong liver cancer cell inhibiting activity.
CN1813758A Levofloxacin hydrochloride micro-pill capsule and its preparing method The present invention relates to a levofloxacin hydrochloride micropill capsule and its preparation method. It is composed of capsule external shell and micropill, the micropill is formed from levofloxacin hydrochloride, blank pill core and adhesive, every pill contains (by wt%) 10%-80% of levofloxacin hydrochloride, 15%-60% of medicine micropill pill core and 5%-30% of adhesive. Besides, said invention also provides the concrete steps of its preparation method.
CN101199532A Methanesulfonic acid reboxetine controlled-release capsule and preparing method thereof The invention relates to a mesylate reboxetine sustained release capsule, which is filled by an active component of mesylate reboxetine, blank core and sustained-release pellets of sustained release preparation. Wherein, according to the weight ratio, the components of the sustained-release pellets are as following: the mesylate reboxetine is 2.61 to 5.22, the blank core is 100, and the sustained release preparation is 2.0 to 100. The invention also relates to a method of preparing the mesylate reboxetine sustained release capsule. The mesylate reboxetine sustained release capsule provided by the invention can avoid the peak and the valley of plasma concentration which occur after the patient takes the ordinary tablets and capsules, can keep balanced and abiding effective plasma concentration with equal flocculent dosage and time interval, can increase curative effect, can improve the bioavailability, can also reduce the intake while keeping the equal plasma concentration to reduce the side effect, and can also improve the compliance of the patients.
CN101768147B Chrysin and substituted salicylate composites, manufacturing method thereof and use thereof The invention discloses novel chrysin and substituted salicylate composites having a general formula below. In the formula, R1 represents CH3 or CH2CH3, R2 represents H and OCH3, R3 represents H, Cl, Br or CH3, and R4 represents H, F, Cl, Br, OH or CH3. The novel chrysin and substituted salicylate composites of the invention have an obvious inhibiting effect on mouse lymphocyte proliferation caused by ConA. In the invention, compounds with high activity are screened out to be used in tests on mouse lymphocyte proliferation caused by anti-CD3 and anti-CD28 antibodies, and the results of the tests show that the compounds can inhibit the mouse lymphocyte proliferation caused by the anti-CD3 and anti-CD28 antibodies in a dose-dependent manner and have the same inhibiting effect with a cyclosporin A positive medicament. Therefore, the compounds are potential nonsteroidal antiinflammatory drugs. The invention discloses a method for preparing the novel chrysin and substituted salicylate composites.
US20120046292 Diacylethylenediamine compound [Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.
US20120270876 Treatment of Conditions Through Pharmacological Modulation of the Autonomic Nervous System Methods are provided for treating a subject for a condition caused by an abnormality in the subject's autonomic nervous system. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is pharmacologically modulated with at least one beta-blocker in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, where such conditions include various disease conditions. Also provided are systems and kits for use in practicing the subject methods.
US7550628 Process for preparing phenolic acid salts of gabapentin The present invention provides a novel process for preparation of the tannate salt of gabapentin for human and veterinary pharmaceutical use. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. However, the prior art neither discloses nor suggests the preparation of gabapentin tannate. The process for preparing gabapentin tannate includes the mixing of gabapentin and tannic acid together in the presence of one or more solvents. The method may further include the step of selecting the one or more solvents from a group consisting of purified water, ethanol, glycerin, propylene glycol, diethylether, methylene chloride, acetone, isopropyl alcohol and mixtures thereof. The process may also include the steps of isolating and purifying the tannate salt. This may be accomplished by filtration, drying, centrifugation and lyophilization. The process may utilize either natural or synthetic tannic acid.
CN101703501B Propargyl imine compounds and use thereof in preparation of MAO inhibitor The invention provides use of propargyl imine compounds in the preparation of a monoamine oxidase inhibitor and new propargyl imine compounds. The propargyl imine compounds have a structural formula (I). The invention has the advantages that: (1) equipment required for the preparation of the propargyl imine compounds is simple, the operation process is simple and convenient, the raw material sources are commercialized and readily available and the compounds serving as the monoamine oxidase inhibitor are stable in nature and high in purity (over 99 percent); and (2) compared with the traditional monoamine oxidase inhibitor, the monoamine oxidase inhibitor prepared from the new propargyl imine compounds has a simpler structure, a higher inhibition activity, higher MAO-A selectivity and higher MAO-B selectivity.
CN101965339A Novel catechol derivative, pharmaceutical composition containing the same, use of the catechol derivative, and use of the pharmaceutical composition Disclosed is a compound represented by the general formula (I), which has a strong COMT inhibitory effect, or a pharmacologically acceptable salt thereof. Also disclosed are a pharmaceutical composition containing the compound or a pharmacologically acceptable salt thereof, and uses of the compound, a pharmacologically acceptable salt of the compound and the pharmaceutical composition. [In the formula (I), R1 and R2 respectively represent a hydrogen, a lower acyl, a lower alkoxycarbonyl or the like,R3 represents a halogenated lower alkyl, a lower acyl, a halogenated lower alkylcarbonyl, a cycloalkylcarbonyl, an optionally substituted arylcarbonyl, a lower alkoxycarbonyl or the like,and R4 represents a lower alkyl, a halogenated lower alkyl, a cycloalkyl, a lower alkoxy-lower alkyl or the like].
US6852695 For therapy of hyperglycemic disorders A water soluble extract of M.charantia named MC6, methods for its preparation and methods for its use in the treatment of hyperglycemic disorders are provided. The active MC6 is characterized by moving as a single band on SDS-PAGE having a molecular weight of less than 10 kDal, and by comprising three peptides. Also provided is a peptide component of MC6 named MC6.1, as well as analogues and mimetics thereof. The active MC6, MC 6.1, MC6.2, and MC6.3 exhibit hypoglycemic activity, even following oral administration. Also provided are methods of using the active agents to treat hyperglycemic disorders, particularly diabetes, where the active agents are preferably orally administered.
EP1682135B1 salt of a tetrahydropyranyl cyclopentyl tetrahydropyridopyridine derivative as CCR2-antagonist The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-e n-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine.
US20060171901 Treatment of malodour This invention relates to methods for inhibiting growth of anaerobic bacteria, particularly halitosis causing bacteria. The methods use BLIS-producing Streptococcus salivarius strains, extracts thereof, and compositions comprising same in the prevention or treatment of halitosis.
CN101627988B Application of structure modified products of salvianolic acid B in pharmacy The invention relates to novel application of structure modified products of salvianolic acid B in pharmacy. The structure modified products of the salvianolic acid B can obviously inhibit the rise of CK and LDH in blood serum, obviously reduce MDA level and improve SOD activity, has effects of resisting oxidation and removing oxygen radical, can improve the condition of myocardial ischemia to obviously relieve the illness state of miocardial infarction, can obviously prolong the time for forming thrombus, and can be applied in preparing medicaments for resisting the myocardial ischemia, medicaments for protecting myocardial ischemia-reperfusion cardiac microvascular endothelial cells, medicaments for resisting cerebral ischemia, medicaments for resisting atherosclerosis, medicaments for resisting the thrombus, anti-ageing medicaments, antitumor medicaments, and medicaments for resisting liver injury and liver fibrosis. The novel application has the advantage that: the application range of the structure modified products of the salvianolic acid B in pharmacy is determined, so that the preparation of the novel medicaments of which the pharmacological activity and bioavailability are higher than those of the salvianolic acid B is possible.
CN1586467A Troxerutin powder injection The troxerutin powder for injection includes troxerutin 2-100 wt% and excipient 0-98 wt%, and the excipient is one of mannitol, lactose, glycine, sorbic alcohol, low molecular weight dextran, glucose, cane sugar and hydrolysate gel. It is bacteria-free powder or bacteria-free freeze dried produce. The present invention is used in treating ischemic cerebral vascular diseases, central retinitis, arteriosclerosis, thrombotic phlebitis, varicosity, etc. and has the advantages of stability, fast dissolution in water and high safety.
DE102007016283A1 Deoxy-D-glucose for producing drug for therapy of arteriosclerosis and arteriothrombosis, particularly for plaque structure in vessel, for preventing or treating restenosis, and for use with compound for continuous release The 2-deoxy-D-glucose. - ACTIVITY : Antiarteriosclerotic; Anticoagulant; Thrombolytic; Vasotropic. - MECHANISM OF ACTION : None given.
WO2013057944A1 Novel spiroindoline compound, and medicinal agent comprising same The present invention provides a novel compound represented by general formula (1), which has an activity of activating glucokinase occurring in the liver and a pancreatic β cell and is useful as a prophylactic and/or therapeutic agent for diseases associated with hyperglycemia, e.g., diabetes. A spiroindoline compound represented by general formula (1) [wherein the ring A represents a nitrogenated 5- to 10-membered heteroaryl group; R1 and R2 may be the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a halo-C1-6-alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group which may have a substituent, a C2-6 alkenyl group which may have a substituent, or the like; R3 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, or the like; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group which may have a substituent, or the like], a salt of the compound, or a solvate of the compound or the salt.
CN101816656A Formula of vinegar powder soft capsules The invention provides a formula of vinegar powder soft capsules. The vinegar powder soft capsules consist of content and capsule shells, wherein the content is comprised of vinegar powder, vegetable oil and lecithin in a weight ratio of 5-7:12-14:0.8-1.2; and the capsule shell material is comprised of gelatin, glycerol and water in a weight ratio of 0.9-1.1:0.35-0.4:0.9-1.1. The vinegar powder may be any table vinegar dry powder such as mature vinegar, rose vinegar and other vinegars containing r-aminobutyric acid, niacin and ligustrazine ingredients and/or a lovastatin ingredient, and the vinegar powder is sieved by a 200 to 300-mesh sieve. The vegetable oil of the invention may be one or a mixture of several of soybean oil, maize germ oil, olive oil, peanut oil and other vegetable grease which can be used in the production of soft capsules. The formula of the vinegar powder soft capsules is favorable for the production of the health-care effect of the vinegar powder and makes the administration of the soft capsules convenient.
US20060009422 Antibiotics incorporating borinic acid complexes; (bis(3-chloro-4-methylphenyl)boryloxy)(3-hydroxypyridin-2-yl)methanone; Antiinflammatory drugs; enhanced stability Methods of treating and/or preventing surface infections, such as acne, in an animal, such as a human being, using antibiotics incorporating borinic acid complexes, especially picolinic acid derivatives, are disclosed, along with compositions of these antibiotics.
CN101590008A Composition preparation of 24-methylene cycloartenol feruloyl esterase and purification process thereof The invention discloses a composition preparation of 24-methylene cycloartenol feruloyl esterase, and a purification process thereof. The purity of 24-methylene cycloartenol feruloyl esterase purified by the purification process can reach more than 80%. The composition disclosed by the invention contains 24-methylene cycloartenol feruloyl esterase and surface active agent, wherein, the surface active agent is selected from Tween 80, polyethylene glycol 400 or mixture thereof. Meanwhile, the invention also discloses an injection of the composition, in particular to freeze-dry powder injection for injection.
EP2450359A2 (R)-N-Methylnaltrexone This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.
WO2008076373A1 Breast cancer therapy based on hormone receptor status with nanoparticles comprising taxane The present invention relates to methods and kits for the treatment of breast cancer based on hormone receptor status of progesterone receptor and estrogen receptor comprising the administration of a taxane alone, in combination with at least one other and other therapeutic agents, as well as other treatment modalities useful in the treatment of breast cancer. In particular, the invention relates to the use of nanoparticles comprising paclitaxel and albumin (such as Abraxane®) either alone or in combination with other chemotherapeutic agents or radiation, which may be used for the treatment of breast cancer which does not express estrogen receptor and/or progesterone receptor.
US20110251158 Fullerene therapies for inflammation and inhibition of build-up of arterial plaque Described herein are methods for treating inflammatory disorders or for inhibiting the build-up of arterial plaque. The methods comprise administering to a subject in need thereof a therapeutically effective amount of a synthetically modified fullerene.
US20080279912 Use of Cis-Epoxyeicosatrienoic Acids And Inhibitors of Soluble Epoxide Hydrolase to Alleviate Eye Disorders The invention provides methods for alleviating eye disorders due to increased intraocular pressure (“IOP”) or inflammation by administering to the eye or eyes of an individual in need thereof a cis-epoxyeicosatrienoic acid, an inhibitor of soluble epoxide hydrolase (sEH), or both. The invention further provides for reducing IOP or inflammation by methods in which the sEH inhibitor or EETs, or both, are administered systemically. In some embodiments, the methods comprise administering to the individual a nucleic acid encoding an inhibitor of sEH.
WO2012002921A1 Multiple dosage forms comprising fenofibrate or fenofibric acid in combination with hmg co a reductase inhibitors such as statins The present invention relates to pharmaceutical formulations comprising a HMG-CoA reductase enzyme inhibitor and a fibric acid derivative in order to be used in the treatment of hyperlipoproteinemia, hypertriglyceridemia, hypercholesterolemia, myocardial infarction and stroke and/or related diseases.
WO2013087744A1 Pyrazolopyridine derivatives, preparation process therefor and therapeutic use thereof The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.
US20060172999 2-[(1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-phenyl-tetrahydropyran-4-yl]methyl-2-oxa-8-aza-spiro[4,5]decan-4-ol; neurokinin 1 (NK-1) receptor antagonists; antidepressant, anxiolytic, analgesic, antiinflammatory agent; migraine, emesis or postherpetic neuralgia The present invention relates to the compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and W are as defined herein, and pharmaceutically acceptable salts thereof; the compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
US20080206293 Absorbent substrate with a non-leaching antimicrobial activity and a controlled-release bioactive agent. This invention relates to antimicrobial wound dressings having a non-leaching antimicrobial activity, releasable antimicrobial and antiprotease agents, and a controlled-release bioactive agent such as doxycycline. The Wound dressing material is absorbent and acts as a substrate for antimicrobial and antiprotease agents as well as bioactive agents. More generally, this invention relates to methods and compositions for materials having a non-leaching coating that has antimicrobial properties. The coating is applied to substrates such as gauze-type wound dressings, powders and other substrates. Covalent, non-leaching, non-hydrolyzable bonds are formed between the substrate and the polymer molecules that form the coating. A high concentration of anti-microbial groups on multi-length polymeric molecules and relatively long average chain lengths, contribute to an absorbent or superabsorbent surface with a high level antimicrobial efficacy. Utilization of non-leaching coatings having a plurality of anionic or cationic sites is used according to this invention to bind a plurality of oppositely charged biologically or chemically active compounds, and to release the bound oppositely charged biologically or chemically active compounds from said substrate over a period of time to achieve desired objectives as diverse as improved wound healing to reduction in body odor.
CN101897931A Powder for dispelling mental stupefaction The invention discloses a preparation method of powder for dispelling mental stupefaction, which is realized through the following technical schemes: spraying less quantity of crystal sugar water onto rhizoma coptidis, scutellaria laterifolia, gardenia and radix curcumae; and then placing into a pot to fry for 5 minutes; taking out and naturally airing and grinding into 200 mesh fine powder; and mixing the fine powder with vermilion and bezoar and evenly stirring to obtain finished product powder. The disease can be cured in a few days by using the method.
US20090136497 Methods for inhibiting cutaneous inflammation and hyperpigmentation This invention provides a method of preventing or treating in a subject contact dermatitis which comprises administering to the subject an amount of a compound capable of inhibiting the stem cell factor signaling pathway effective to prevent or treat contact dermatitis so as to thereby prevent or treat contact dermatitis in the subject. This invention also provides a method of preventing or treating in a subject hyperpigmentation, asthma, cutaneous inflammation, anaphylaxis and bronchospasm, mastocytosis, tumors which express activated kit, and conception.
CN1611218A Fixed dose compound preparation of antitubercular drug and its preparing method The present invention relates to an antituberculotic compound preparation containing fixed dosage of rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride. Besides, it also contains proper quantity of disintegrant, binding agent, lubricant, dilutent and water-soluble coating powder. Its preparation method includes the following steps: sieving rifampicin with sieve with 100 meshes, sieving other materials with sieve with 60 meshes, adding binding agent, disintegrant and dilutent, mixing them uniformly, dry granulating, mixing theo btained granules with disintegrant and dilutent uniformly, then tabletting so as to obtain the invented product antituberculotic compound preparation with high therapeutic effect.
US20080242728 gabapentin tannate to treat central nervous system disorders; used in sustained release applications and to improve certain organoleptic properties such as taste The present invention relates to pharmaceutical compositions of gabapentin tannate in solid dosage form, processes for production of those compositions and methods of use of those compositions. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. The process may utilize either natural or synthetic tannic acid.
CN101164594A Paste suitable for fundus disease and retinal microcirculation disease and preparation method thereof The present invention relates to an ointment preparation for curing pathologic change of eye fundus and pathologic change of retinal microcirculation and its preparation method. Said ointment preparation is made up by using black pearl extract, deep-sea truff and euthynnus yaito body interior extract DHA, fat-soluble retinol, phytoanthin, amber, musk, prinsepia seed, rhodiola root, cyperus malaccensis var, brevifolius and epimedium through a certain preparation process. Said invention also provides its concrete preparation method. The invented ointment preparation can be made into as ticking preparation by adding sticking material into the above-mentioned raw material.
US20070254287 Diagnostics and Therapeutics for Diseases Associated with Dipeptidyl-Peptidase 10 (Dpp10) The invention provides a human DPP10 which is associated with the cardiovascular diseases, dermatological diseases, endocrinological diseases, metabolic diseases, cancer, inflammation, gastroenterological diseases, hematological diseases, respiratory diseases, muscle skeleton diseases, neurological diseases, urological diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular diseases, dermatological diseases, endocrinological diseases, metabolic diseases, cancer, inflammation, gastroenterological diseases, hematological diseases, respiratory diseases, muscle skeleton diseases, neurological diseases, urological diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of DPP10 as well as pharmaceutical compositions comprising such compounds.
US6887997 Tricyclic analogues of guanosine, a nucleobase for treating tumor Fused tri-heterocyclic compounds of formula: R1 is H or alkyl; R2 is H, alkyl, alkenyl, aryl, heteroaryl, cyclyl, or heterocyclyl; R3 and R4, independently, is H, alkyl, alkenyl, aryl, heteroaryl, cyclyl, heterocyclyl, or (CRaRb)mX(CRcRd)nY; in which X is a bond, O, S, or NRe; Y is alkoxy, aryloxy, heteroaryloxy, OC(O)Re, C(O)Re, N(ReRe′), NReC(O)Re′, S(O)2Re, or SRe; each of m and n, independently, is 1, 2, 3, 4, or 5; each of Ra, Rb, Rc, Rd, Re, and Re′, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; and R5 is H or halogen.
US20120148584 Vegf-specific antagonists for adjuvant and neoadjuvant therapy and the threatment of early stage tumors Disclosed herein are methods of treating benign, pre-cancerous, or non-metastatic tumors using an anti-VEGF-specific antagonist. Also disclosed are methods of treating a subject at risk of developing benign, pre-cancerous, or non-metastatic tumors using an anti-VEGF-specific antagonist. Also disclosed are methods of treating or preventing recurrence of a tumor using an anti-VEGF-specific antagonist as well as use of VEGF-specific antagonists in neoadjuvant and adjuvant cancer therapy.
CN103479656A Application of saikoside d in preparation of anti-hepatic fibrosis disease drugs The invention discloses application of saikoside d in preparation of anti-hepatic fibrosis disease drugs, and belongs to the technical field of medicines. The invention aims to provide pharmacological activities exhibited by the saikoside d in treatment of hepatic fibrosis symptoms and related mechanisms. The saikoside d has a good anti-hepatic fibrosis effect, and the action mechanisms may be related with improvement of activities of superoxide dismutase, reduction of generation of oxyradical and inhibition of activation of TGF-beta 1 (transforming growth factor) signaling pathway.
WO2009144240A1 Composition and method for the assay and treatment of anthrax A method for the treatment and/or prophylaxis of infection of a subject with Bacillus anthracisis provided wherein the method comprises the step of administering to the subject a therapeutically effective amount of a heavy chain camelid antibody,or an antigen binding portion thereof,which has a binding specificity for at least one Bacillus anthracis protein. Preferably, the Bacillus anthracis protein is a toxin protein selected from the group consisting of protective antigen, lethal factor and edema factor.In certain embodiments, the method further comprises the step of administering a therapeutically effective amount of an antibiotic to the subject. Also provided is an isolated heavy chain camelid antibody, or an antigen binding portion thereof, which has a binding specificity for at least one Bacillus anthracis protein.
US7214713 Supplement with anticancer properties with fermentation of carbohydrates with biosynthesis of Penicillum A food supplement having prophylactic and-cancer effects, wherein the supplement comprises 20 to 99.99% by weight of a product of biosynthesis by the productive microorganism Penicillium oxalicum var. Armeniaca CCM 8242, obtained by fermentation of a nutrient broth containing carbohydrates and ammonia nitrogen, and 0.01 to 8′% by weight of a physiologically inert carrier, and optionally auxiliary additives.
US20090233986 Methods and compositions for using sax2 The present invention is generally directed to factors involved in energy metabolism. More specifically, a new gene is identified and shown to be a homeobox Sax2 gene that is involved with an obesity phenotype. Deletion of the causes growth retardation starting at birth and high postnatal lethality. Further, abrogation of the gene leads to a lack of fat accumulation in white adipose tissue and brown adipose tissue, as well as low blood glucose levels. Methods and compositions for making and using the product of the gene as well as for the manufacture of medicament for the treatment of obesity and obesity-related disorders are described.
US20100234473 Process for preparation of 3-(2-hydroxy-5-substituted phenyl)-n-alkyl-3-phenylpropylamines A new process for preparation of 3-(2-hydroxy-5-substituted phenyl)-N,alkyl-3-phenylpropylamines from cinnamyl chloride via N-alky-3-phenylprop-2-en-1-amine has been developed.
CN103113216A Naproxen sodium crystal compound, medical composition and preparation method thereof The invention relates to a naproxen sodium crystal compound and a medical composition comprising the naproxen sodium crystal compound, and in particular relates to a powder-injection and a preparation method thereof. The naproxen sodium crystal compound is superior to other marketed products in stability and solubility, high in purity, easy to industrialize and suitable for preparing pharmaceutical preparations, and in particular suitable for long-time storage.
CN102643252A Piperazinoacethydrazide-containing diarylurea derivatives and application thereof The invention belongs to the technical field of medicine, and relates to piperazinoacethydrazide-containing diarylurea derivatives and application thereof for preparing antineoplastic drugs, particularly piperazinoacethydrazide-containing diarylurea derivatives, a pharmaceutical composition using the derivatives as active components, and application thereof for treating and/or preventing various cancers. The structural general formula of the compounds is disclosed as follows.
US20070274910 e.g. 3-[2-(2-Aminophenyl)ethyl]-8-benzyl-7-(2-methylamino)ethyl-1-propylxanthine; A1-adenosine receptor antagonist; antiallergen, antiinflammatory agent; AIDS and immune deficiency disorders, asthma; good water solubility This invention relates to compounds of formula (I): wherein R1 is a branched or straight chain C1-C6 alkyl; R2 is of the formula (II), wherein n is an integer ranging from 1 to 8; R5 is H or (CH2)pCH3, and R6 is H or (CH2)mOH, wherein p is an integer ranging from 1 to 7 and m is an integer ranging from 1 to 8; R3 is of the formula (III), wherein q is an integer ranging from 1 to 8; and R7 is selected from the group consisting of H, OH, NH2, (CH2)tOH, and R9COOH; wherein R9 is a straight or branched chain alkylene or alkenylene group having 1 to 8 carbon atoms, and t is an integer ranging from 1 to 8; R4 is of the formula (IV), wherein r is an integer ranging from 1 to 8 and R8 is selected from the group consisting of H, OH, (CH2)fNH2, (CH2)sOH, and R10COOH; wherein f is 0 or f and s are independently integers ranging from 1 to 8; and, R10 is a C1-C8 straight or branched chain alkylene or alkenylene; and; salts, solvates, and hydrates thereof. The present invention further provides methods of preparing the compounds of formula (I) and their use as therapeutic agents and diagnostic agents.
WO2008109532A3 Nucleic acid compounds for inhibiting fas gene expression and uses thereof The present disclosure provides meroduplex ribonucleic acid molecules (mdRNA) capable of decreasing or silencing FAS gene expression. An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to a FAS mRNA. In addition, the meroduplex may have at least one uridine substituted with a 5-methyluridine, a nucleoside replaced with a locked nucleic acid, or optionally other modifications, and any combination thereof. Also provided are methods of decreasing expression of a FAS gene in a cell or in a subject to treat a FAS-related disease.
US20100272639 Polysaccharide nanoparticles Polysaccharide nanoparticles that are particularly useful in for example drug and agent delivery, tissue-specific targeting, for medical imaging and diagnosis, as well as modifiers of physico-chemical properties. The nanoparticles can be highly-branched glucose homopolymers and can be characterized by a uniform spherical shape. They are monodisperse, hydrophilic and produce low solution viscosities. The nanoparticles are non-toxic, biocompatible and biodegradable. Also, the process of isolation of said polysaccharide nanoparticles from various organisms including, but not limited to, microorganisms such as bacteria and yeasts. Also provided are methods for chemical conjugation of the polysaccharide nanoparticles with various agents. Also provided are examples of use of the polysaccharide nanoparticles and their derivatives as drug delivery systems and fluorescent di-agnostics.
CN101804051A Liposome injection of pharmaceutical composition of amoxicillin sodium and clavulanate potassium The invention provides a liposome injection of a pharmaceutical composition of amoxicillin sodium and clavulanate potassium, which consists of amoxicillin sodium, clavulanate potassium, a liposome carrier, a lyoprotectant and a freely optional antioxidant, wherein the liposome carrier is egg yolk phosphatidylinositol and sodium taurocholate. The liposome injection has good preparation stability, liposome can avoid the fracture due to dehydration, fusion, ice crystal generation and the like during the freeze-drying process, and the liposome can still keep the good encapsulation rate after hydration and redissolution.
US6888001 Selective modulators of the nicotinic acetylcholine receptor useful in the treatment of pain, Alzheimer's disease, memory loss or dementia or loss of motor function. The present invention provides compounds of the formula: wherein m is 0, 1 or 2; p is 0 or 1; Y is O, S, S(O) or S(O)2 and R1 to R7 are various substituents as selective modulators of the nicotinic acetylcholine receptor useful in the treatment of pain, Alzheimer's disease, memory loss or dementia or loss of motor function.
EP1330246B1 Use of hydroxyeicosatetraenoic acid derivatives in intraocular surgery The use of HETE derivatives in intraocular surgery (e.g., cataract surgery) is disclosed. The HETE derivatives protect and maintain the corneal endothelium.
US7309497 Injectable pharmaceutical composition for systematic administration of pharmacologically active ingredients The invention relates to novel pharmaceutical compositions for the systemic administration of pharmacologically active ingredients. The invention relates in particular to an injectable pharmaceutical composition comprising (a) a pharmacologically active ingredient in a solid phase, (b) a vehicle consisting substantially of polyol fatty acid esters with a degree of esterification of over 80%, and (c) a wetting agent consisting substantially of polyol fatty acid esters with a monoester proportion of over 60%. The inventive composition is used for the systemic administration of numerous pharmacologically active ingredients, whereby the ingredients are released from the pharmaceutical composition over a period of at least 12, preferably at least 24 hours.
EP1564292A1 Pharmaceutical compositions and methods of treatment based on VEGF antisense oligonucleotides This invention relates to compositions and methods for inhibition of abnormal proliferation of cells or angiogenesis. More particularly this invention provides VEGF antisense oligonucleotides capable of inhibiting proliferation of cancer cells or angiogenesis or combinations thereof.
WO2012107356A1 Aqueous pharmaceutical composition for preventing and/or treating allergically irritated nasal mucosa and use thereof The invention relates to an aqueous pharmaceutical composition, which comprises an anti-inflammatory and/or antiallergic agent, oil, and at least one viscosity regulator. The invention further relates to the use of said pharmaceutical composition for preventing and/or treating allergically irritated nasal mucosa.
CN103709280A Mucoadhesive polymers having vitamin B partialstructures The mucoadhesive properties of polymer compounds can be considerably improved by the covalent binding of thiol partial structures to said compounds, because as a result disulfide bridge bonds are formed having mucus glycoproteins. By converting the free thiol groups on such polymers into disulfides having mercaptonicotin amides or mercaptopyridoxines, said thiol groups become comparatively more reactive, so that the mucoadhesive properties of said polymers are considerably higher. In addition, polymers that comprise the disulfide partial structures having mercaptonicotin amides or mercaptopyridoxines do not have to be protected from oxidation and have comparatively higher permeation-accelerating properties.
US7256197 Methods for synthesis of diarylmethanes The present invention relates to dihydrofolate reductase inhibitors having an aromatic group and a heteroaromatic group linked by a methylene group; methods of preparation of dihydrofolate reductase inhibitors that include metal mediated cross coupling of an aromatic halide or heteroaromatic halide with an organozinc reagent; and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such dihydrofolate reductase inhibitors.
CA2799559A1 Production of dha and other lc-pufas in plants The invention provides recombinant host organisms (e.g., plants) genetically modified with a polyunsaturated fatty acid (PUFA) synthase system and one or more accessory proteins (e.g., PPTase and/or ACoAS) that allow for and/or improve the production of PUFAs in the host organism. The present invention also relates to methods of making and using such organisms (e.g., to obtain PUFAs) as well as products obtained from such organisms (e.g., oil and/or seed).
WO2013102249A1 N-phenylpiperazine derivatives that are antagonists of α1a, α1d adrenoceptors and 5-ht1a receptors for the treatment of benign prostate hyperplasia, pharmaceutical compositions containing the same The present invention provided N-phenylpiperazine derivatives for use as multiple binders and/or antagonists of α1A adrenoceptors, α1D adrenoceptors and 5-HT1A serotonin receptors. These substances are candidates to prototypes for the treatment of benign prostate hyperplasia and lower urinary tract symptoms, and are useful in pharmaceutical compositions.
CN103626700A Salt of cyclopropane dicarboxamide derivative The invention relates to a fumarate of N-{3-fluo-4-[(6-(methoxyl)-7-{[3-(4-morpholinyl) propyl] oxy}-4-quinolyl) oxy] phenyl}-N-(4-fluorophenyl)-1, 1-cyclopropyl dicarboxamide (formula I), a preparation method or pharmaceutically acceptable solvates thereof, and application of the fumarate of N-{3-fluo-4-[(6-(methoxyl)-7-{[3-(4-morpholinyl) propyl] oxy}-4-quinolyl) oxy] phenyl}-N-(4-fluorophenyl)-1, 1-cyclopropyl dicarboxamide (formula I) to preparation of medicaments for treating cancer and / or alleviating tumor.
CN102525889A Ornidazole ophthalmic gel and preparation method and application thereof The invention discloses ornidazole ophthalmic gel and a preparation method and application thereof, belongs to the technical field of medicine, and relates to ornidazole serving as an active medicament ingredient. The ornidazole is prepared into the ophthalmic gel for the first time, and the gel is used for preventing and treating blepharitis, hordeolum and conjunctivitis caused by infection of demodex and dry eye syndrome caused by meibomain gland dysfunction and used for preventing and treating infection of acanthamoeba polyphaga and anaerobic bacteria in a corneal contact lens wearing process. The ornidazole ophthalmic gel consists of the ornidazole and a pharmaceutically acceptable carrier, and every 100 grams of ornidazole ophthalmic gel contains 0.1 to 3.0 grams of ornidazole.
CN1883285A Compound sleep assistant health product The invention provides a health product of compound recipe for solving the problem of insomnia for the middle-aged and elder people, wherein a formulation is disclosed to realize substantial actions for tranquilization, longevity extension and other health care effects.
CA2545364A1 Methods of modulating angiogenesis and cancer cell proliferation Methods for regulating angiogenesis by modulating the activity of 20-HETE are disclosed. Further disclosed are methods of inhibiting cancer and tumor cell growth by exposing the cancer and tumor cells to 20-HETE inhibitors.
CN103450194A Tetrahydro-beta-carbolinyl-3-formyl aliphatic chain amines, and preparation, nano structure, immunosuppression action and application thereof The invention relates to 6 aliphatic chain amine modified carbolinyl carboxylic acid analogs disclosed as general formula I, wherein n is equal to 6, 8, 10, 12, 14 or 16. The invention also relates to a preparation method of the 6 aliphatic chain amine modified carbolinyl carboxylic acid analogs disclosed as general formula I. The invention further relates to a nano structure of the 6 aliphatic chain amine modified carbolinyl carboxylic acid analogs disclosed as general formula I. By researching the inhibiting action of the saturated fatty chain amine modified carbolinyl carboxylic acid analogs on the spleen lymphocyte mitogen breeder reaction and the survival time after transplanting the mouse postotic cardiac muscle, the invention further relates to excellent immunosuppression action of the 6 aliphatic chain amine modified carbolinyl carboxylic acid analogs disclosed as general formula I. The 6 aliphatic chain amine modified carbolinyl carboxylic acid analogs with immunosuppressive activity disclosed as general formula I have wide application prospects in preparing immunosuppressive drugs.
CN101926763A Method for preparing lipoalprostadil sterile preparation The invention provides a method for preparing lipoalprostadil sterile preparation. The rotating sterilization technique is applied to the method for preparing lipoalprostadil for the first time. The method comprises the steps of using the rotating sterilization technique to sterilize an encapsulated lipoalprostadil Cillin-glass bottle, and in the process of sterilization, keeping the sterilizing temperature between 128 and 134 DEG C, maintaining the pressure between 165 and 210 kPa, and keeping for 300 to 600 seconds. The method of the invention can efficiently prevent the basic drug of the lipoalprostadil from degrading caused by traditional steam sterilization technique so as to meet the demand of sterilization.
WO2008090201A1 Use of folic acid, vitamin b6, and vitamin b12 The present invention relates to the use of folic acid, vitamin B6, and vitamin B12, for the preventive and acute treatment of osteoporosis. The invention describes, in particular, pharmaceutical agents and nutritional supplements with a corresponding combination of active ingredients, and agents in the form of commercial packages with corresponding combined preparations or monopreparations for combined use.
EP1809632A2 Pyrazolo[4,3-d]pyrimidine derivatives useful as pde-5 inhibitors This invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5 and R5 and R6 are as described herein,which are cyclic guanylate monophosphate (cGMP)-specific phosphodiesterase type 5 inhibitors (PDE-5 inhibitors) that are useful in the treatment of hypertension and other disorders, to processes for their preparation, intermediates used in their preparation, to compositions containing them and the uses of said compounds and compositions.
US20120264710 Systems and Methods for Detecting hENT1 Expression in Hematological Disorders This invention relates generally to methods, assays and systems for detecting hENT1 expression levels in hematological disorders, to methods, assays and systems for detecting hENT1 expression levels in hematological disorders using flow cytometry, and to methods, assays and systems for detecting hENT1 expression levels in myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML) using flow cytometry. The invention also relates to diagnostic and therapeutic uses for the detection of hENT1 expression levels in a subject.
CN101919850A Enteric slow release preparation containing S-ketoprofen and omeprazole used as active components, as well as preparation method and application thereof The invention relates to an enteric slow release preparation containing S-ketoprofen and omeprazole used as active components, as well as a preparation method and application thereof. The omeprazole is an enteric pellet, and the S-ketoprofen releases a medicament through a slow release framework. The invention discloses the preparation method and the application of the enteric slow release preparation.
EP2294057A1 PROCESS FOR PREPARING A CRYSTALLINE FORM COMPOUND OF 3-BENZYL-2-METHYL-2,3,3a,4,5,6,7,7a-OCTAHYDROBENZO[d]ISOXAZOL-4-ONE A process for preparing a crystalline form compound of 3-benzyl-2-methyl- 2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one is described, comprising the step of reacting 3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4- one and fumaric acid in one or more solvents, wherein at least one solvent is a solvent having a carbon atom number of from 3 to 6, said solvent being non- halogenated and having a dielectric constant ε in the range from 4 to 25. The process of the invention enables to obtain a co-crystal comprising 3-benzyl-2- methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one and fumaric acid.
US20100003349 Portable, nitric oxide generator An apparatus for portable delivery of nitric oxide without the need for pressurized tanks, power supplies, or other devices provides a single therapy session by triggering a heater to heat a reaction chamber. A piercing assembly may trigger to open sealed containers, such as bags, of liquid water or salt water in order to activate the heaters. Upon addition of liquid such as water or salt water to a chemically reactive heating element, heat is generated to activate the chemicals generating nitric oxide within a sealed reactor. Upon triggering, liquid containers are unsealed, the liquid drains down to initiate reaction of the heating chemicals, and the heat begins to penetrate the reactor. The reactor, in turn, heats its contents, which react to form nitric oxide expelled by the reactor to a line feeding a cannula for therapy.
CN101869561A Tacrolimus-containing improved release composition The invention discloses a tacrolimus-containing improved release composition. In vitro dissolution test performed by using 0.1N HCl as a dissolution medium according to the United States Pharmacopoeia stirring paddle method, the active ingredients released in 0.5 hour are less than 20 weight/weight percent; and the bioavailability is improved by effectively reducing or even eliminating the effect of CYP3A4 metabolism. The improved composition can be coated by using an enteric coating, and/or can contain solid dispersoid or solid solution of tacrolimus in a hydrophilic or water-miscible medium and one or more release modifiers, and/or can contain solid dispersoid or solid solution of tacrolimus in an amphiphilic or hydrophobic medium and one or more release modifiers.
WO2011091890A1 A method for post coital contraception in overweight for obese female subjects using ulipristal acetate The invention provides a method for providing post coital contraception in a female subject, comprising providing the subject with a therapeutically effective amount of ulipristal acetate, wherein the female subject is overweight or obese.
CA2447765C 1-biaryl-1,8-napthyridin-4-one phosphodiesterase-4 inhibitors Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are phosphodiesterase-4 inhibitors useful in the treatment of asthma and inflammation.
US20080033018 Therapeutic Agents For Overactive Bladder The present invention provides a therapeutic agent for overactive bladder, which has both a KATP channel opening action and a nitrate-like action and is further expected to produce an ameliorating effect for ensuring a reflexive and suitable cooperation between contraction-relaxation of abdominal/bladder wall muscle and relaxation-contraction movement of urethral sphincter during urination and urine storage, so that the therapeutic agent does not induce oliguria or urinary retention and has no serious side effect. Nicorandil or a pharmaceutically acceptable salt thereof is used as an active ingredient.
CN103142625A Fosfomycin sodium pharmaceutical composition and preparation method thereof The invention provides a fosfomycin sodium pharmaceutical composition and a preparation method thereof, relating to the field of a medicinal preparation and a preparation method thereof. The invention mainly solves the problems of high dosage of single fosfomycin sodium and metronidazole preparation, poor treatment effect after combination, and great side effect in the prior art. The pharmaceutical composition comprises fosfomycin sodium and metronidazole lipid microspheres in a weight ratio of 100:3-100:10, wherein the weight of the metronidazole lipid microspheres is metered on the basis of metronidazole; and when the pharmaceutical composition is prepared into a powder injection, the pH value of the water solution of the pharmaceutical composition is 6.5-7.0. The pharmaceutical composition powder injection provided by the invention has high curative effect, and can reduce the consumption of the metronidazole by more than 80%, thereby greatly relieving or avoiding the toxic and side effects of the metronidazole, especially digestive tract reactions, including nausea, vomit, inappetence, abdominal colic and neurotoxicity, and lowering the incidence rate of adverse reactions.
CN102526066A Separate type water suspension medicament of fluticasone propionate containing auxiliary materials for treating skin disease The invention relates to a separate type water suspension medicament of fluticasone propionate containing auxiliary materials for treating skin disease, composed of separately packed fluticasone propionate and separately packed water, wherein the fluticasone propionate contains one or more kinds of pharmaceutical auxiliary materials for skin, is insoluble in water and has a D90 particle size of 0.1-10mu m.
WO2013106683A1 Methods of treating and preventing cancer by disrupting the binding of copper in the map kinase pathway The present disclosure provides methods of treating and/or preventing cancer in a subject comprising administering to the subject a copper-reduced diet by itself or as a supplement along with a regular diet to create a copper-reduced melieu, maintain a reduced-copper melieu, or both, thereby treating and/or preventing the development of the cancer. Methods also comprise further adding a copper chelator, MEK inhibitor, or combinations thereof.
CN102028934A Taxol complex preparation drug The invention relates to a taxol complex preparation drug. Based on the technical scheme, one part of the taxol complex preparation drug is a taxol anticancer drug capsule, the other part is a cyclosporine A capsule, and the two capsules are pressed together, or the two capsules are wrapped by a layer of capsule after being pressed to form a compound capsule. A preparation method of the taxol complex preparation drug has the following steps of taxol anticancer drug capsule preparation: uniformly mixing taxol active substances and a drug excipient according to the proportion of a taxol anticancer drug, and wrapping the mixture in a capsule; cyclosporine A capsule preparation: uniformly mixing cyclosporin A and a matched excipient according to the proportion of a cyclosporine A drug, and wrapping the mixture in a capsule; preparation of a complex preparation: pressing the capsules prepared in the two steps together, and directly applying; or wrapping the two capsules with a layer of capsule after being pressed to form the compound capsule. The invention has the advantages of mature production, convenience in orally taking, easier quality control and good anticancer therapeutic efficacy.
US7064133 A 2-carbamoyl-8-hydroxyquinoline-7-carboxylic acid compound or its salt, e.g., 2-(3,4-dihydroxybenzylcarbamoyl)-8-hydroxyquinoline-7-carboxylic acid or its sodium salt, useful as a retrovirus integrase inhibitor, especially for treatment of HIV The invention relates to derivatives corresponding to formula I: in which X is an alkyl-(CH2)n— chain with n=0, 1 or 2, or O or N, Z is an aromatic which may contain heteroatoms chosen from O, N or S, as substitutions for the carbon atoms constituting said aromatic ring, this ring being substituted or otherwise with Rb, Rb represents 1 to 3 substituents chosen from —OH, —OR, —COOH, —COOR, —COH, —COR, —NH2, —NH(R), —NH(R,R′), —SH, —SR and CN, Ra is H or —(CH2)n′—Y, with n′=0, 1, 2 or 3 and Y and —CH3, —COOH, —COOR, —CN, —OH, —OR, SR, or an aryl group optionally substituted with Rb, R and R′ represent a linear or branched alkyl chain of 1 to 4 C, and their pharmaceutically acceptable salts. Application as active ingredient of medicaments inhibiting retrovirus integrases.
EP2785379A1 Peptide-mediated delivery of active agents across the blood-brain barrier Provided herein are methods for transporting an active agent (e.g., a therapeutic agent or an imaging agent) across the blood-brain barrier (BBB) in a patient. For example, the methods provided herein can be used to treat a brain disease in a patient, such as brain cancer. In some embodiments, the methods provided herein can be used to image the central nervous system of a patient.
US20090062234 Substituted organopolysiloxanes and use thereof The invention relates to new compounds of Formula (1): wherein Q is selected from CXYR′ and RC(Z) wherein Z is selected from oxygen, hydrogen, OH, NR2 and NNR2R3, and wherein X and Y are each selected from hydrogen, RC(Z), CN or C(O)W and W is selected from OH, OR6, O(M+″)1/″ and NR2R3 and R, R′, R2, R3 and R6 are each selected from hydrogen, an optionally substituted linear or branched group selected from C1-40-alkyl, C2-40-alkenyl, C2-40-alkynyl group, an aryl and C1-40-alkylaryl group and M is a metal ion derived from a lanthanide, actinide, main group or transition metal and V is selected from an optionally substituted linear or branched group selected from C1-40-alkyl, C2-40-alkenyl, C2-40-alkynyl group, an aryl group, a C1-40-alkylaryl, sulfide, sulfoxide, sulfone, amine, a polyalkyl amine, a phosphine or other phosphorous containing group; and n is an integer from I to 4. The free valences of the silicate oxygen atoms are saturated by one or more of silicon atoms of other groups of Formula 1, hydrogen, a linear or branched C1-12-alkyl group or by end groups R4 3M′01/2, cross-linking bridge members or by polymer chains of R4 gM′(OR)mOw2 or Al(OR5)3-POP/2 or R4AI(OR5)2_,0,/2; where M is Si or Ti; R5 is a linear or branched C1-12-alkyl group or an aryl or C1-40-alkylaryl group; and R4 is a linear or branched C1-12-alkyl group or an aryl or C1-40-alkylaryl group; k is an integer from I to 3 and q and m are integers from 0 to 2; such that m+k+q=4; p is an integer from I to 3; and r is an integer from 1 to 2. The compounds are useful as scavengers for the removal of unwanted organic and inorganic compounds, for solid phase extraction, for solid phase synthesis, for the immobilisation of bio-molecules, as ion exchanger materials, as catalysts and catalyst supports and as chromatography materials.
US20120322800 Sepiapterin Reductase Inhibitors For The Treatment of Pain Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).
CN1919191A Application of ring icariine in the preparation of medicine for preventing and treating organ transplantation rejection The invention discloses an immune inhibiting drug and application based on ring-icariin in the formula I, which is characterized by the following: inhibiting immuse exclusive reaction in the organ transplanting course, modifying transplanted organ function.
CN101138575A Prescription of chrysanthemum lozenge having functions os getting rid of the hot temper and beneficial to one's eyes The invention relates to a health food product, in particular to a recipe of wye chrysanthenum buccal tablet with healthy function of clear vision and refreshment. The invention takes wye chrysanthenum, one of the four special local wye medicines, as main raw material. The invention is made of an extracted liquid of wye chrysanthenum, mint ice, sugar, dextrin and starch through the procedures of extraction, granulation, drying and pressing. The use of the product proves that the invention with the functions of clear vision and refreshment, influenza prevention and disease-resistant ability is a health food product for subhealth crowd.
US20080234385 Method For Inhibiting Tnf-Alpha The present invention encompasses methods for inhibiting TNF-alpha expression with N-substituted dopamine derivatives. In this method a cell is administered a pharmaceutically effective amount of N-acetyl dopamine derivatives or N-alkyldopamine derivatives and a pharmaceutically acceptable carrier for treating a cell, preferably in an animal or human suffering from overexpression or abundant TNF-alpha. The N-acetyldopamine derivative or N-alkyldopamine derivatives may be administered alone or in combination with N-acetylserotonin (NAS) or other compound to inhibit TNF-alpha expression. Also disclosed is a method of treating a TNF-alpha related disease and/or disorder using such a compound.
CA2191664C Formulation for iron chelation, a process for preparing the formulation and a method of treating thalassemia A pharmaceutical formulation useful for treating patients suffering from thalassemia, which comprises powder of Anemonin Pretensis in an amount in the range of 0.02 to 0.12 wt % of the formulation, quinine sulphate in an amount in the range of 0.0005 to 0.003 wt % of the formulation, distilled or demineralised water in an amount in the range of 0 to 40 wt % of the formulation, and ethanol in an amount in the range of 99.88 to 60 wt % of the formulation; and a process for preparing the formulation by mixing the above ingredients.
WO2011084962A1 Analogs of dehydrophenylahistins Analogs of dehydrophenylahistins are disclosed as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.
WO2010083649A1 Bisarylurea derivatives and their use Bisarylurea derivatives of formula I or the pharmaceutically acceptable salts are provided. The compounds of formula I are used for the manufacture of inhibitors of receptor protein tyrosine kinases and medicament for treating and/or preventing a tumor.
US20080131501 enhanced immediate release formulations of topiramate, in which 80% of the active ingredient is released in the period of time of not more than 30 min. These formulations may be advantageously used for the treatment of acute neurological conditions, such as migraine. The present invention provides enhanced immediate release formulations of topiramate, in which 80% of the active ingredient is released in the period of time of not more than 30 min. These formulations may be advantageously used for the treatment of acute neurological conditions, such as migraine.
US20120189655 Attenuated Live Vaccine for Prevention of Porcine Reproductive and Respiratory Syndrome The present disclosure provides an attenuated live vaccine strain and the formulations thereof, for preventing pigs from infection of porcine reproductive and respiratory syndrome (PRRS). The preparation methods for the vaccines and the formulations are also provided. The attenuated live vaccine strain provided herein offers significant immunological protection to pigs against PRRS. The vaccine formulations of the present disclosure also have advantages in long shelf lives as well as good stability during storage.
US20120115867 New class of histone deacetylase inhibitors This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen or C1-C6 alkyl, R3, R4 are, independently, hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl or C1-C6 haloalkoxy, and R5 and R6 are as further defined in the specification, and pharmaceutical acceptable salts thereof.
US7258872 Chromone enteric release formulation Orally administered chromones have been found to be effective in the treatment of allergic conditions such as asthma, general food allergies, ulcerative colitis, atopic eczema, chronic urticaria, and irritable bowel syndrome if it is presented such that the respective chromone becomes bioavailable within ten minutes of exposure to an intestinal fluid.
EP1809620B1 Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors The present invention relates to new tetrazole compounds of formula I wherein B, P, Q, W, Rl and R2 are defined in the description: invention compounds are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
US20110014210 Chlamydia vaccine Compositions and methods for the treatment of Chlamydial infection are disclosed. The compositions provided include polypeptides that contain at least one antigenic portion of a Chlamydia antigen and DNA sequences encoding such polypeptides. Pharmaceutical compositions, vaccines and diagnostic kits are also disclosed.
US7393543 Vaginally administratable progesterone-containing tablets and method for preparing same The present invention provides a method for preparing a tablet for the vaginal administration of progesterone for systemic use. The method comprises first mixing water with micronized progesterone, the total amount of water mixed with said micronized progesterone not exceeding the maximum wetting capacity of the micronized progesterone, drying the wetted, micronized progesterone; mixing the dry micronized progesterone with other pharmaceutically acceptable excipients or diluents; and; forming a tablet by direct compaction of the dry micronized progesterone. Tablets prepared by this method are also provided.
US20120101125 Substituted isoquinoline derivatives, pharmaceutical compositions, and methods of use as beta-secretase inhibitors The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.
CN101332196A Amoxicillin/clavulanate potassium dispersible tablets and preparation method thereof The present invention discloses an amoxicillin/clavulanate potassium dispersible tablet and a preparation method thereof. The present invention contains amoxicillin/clavulanate potassium and auxiliary materials; the weight proportion of the amoxicillin and the clavulanate potassium is 7:1; the auxiliary materials contain a disintegrant, and one or multiple materials selected from crosslinked carboxymethylcellulose sodium, crosslinked polyvinylpyrrolidone, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, carboxymethylcellulose sodium, carboxymethylcellulose calcium and sodium dodecyl sulfate; calculated by the total weight of the auxiliary materials, the optimally selected carboxymethylcellulose sodium accounts for 10 to 15 parts. The present invention with appropriate selection of auxiliary materials and active medicines for prescription can rapidly disintegrating the dispersible tablet; the dispersible tablet can be totally disintegrated within 3 minutes in 100ml water at 20 DEG minus/plus 1 DEG; the disintegrated particles should all pass through standard II screen for clinical application.
WO2013104871A1 Composition containing agmatine, and uses thereof in preparing drugs or neutraceutical substances The present invention relates to novel compositions including a mixture of cadaverine, putrescine, spermine and spermidine at a concentration varying from 0.31 to 0.63 nmol per gram of composition, said composition also including agmatine at a concentration varying from 120 to 17,100 nmols per gram of composition, and to the uses thereof in treating diseases associated with the hyperproliferation of cells in a patient.
US20130059858 Benzofuranyl analogues as gpr119 modulators Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, where-in A, L, m, n, o, p, R2, R3, R3, R4 and R5 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
CN103655522A Cardiovascular and cerebrovascular diseases and paper patch A large number of domestic and foreign research results and abundant report data and abundant reports data show clearly that periodontal diseases are closely related to cardiovascular and cerebrovascular diseases. People notices that the chief culprit of the cardiovascular and cerebrovascular diseases is in-oral-cavity periodontal pathogen entering into the blood circulation, so that the people puts forward a preventive measure using a strong fungicide to kill the in-oral-cavity periodontal pathogen; but normal bacterium colonies are also killed by the measure, the measure is undesirable. British (Daily Mail) website reports that heart disease and stroke probability can be reduced by frequent tooth brushing. Poor oral hygiene and gum bleeding can lead to as many as 700 kinds of bacteria into the blood, so that 'cleaner oral cavity, healthier heart' is put forward. The applicant thinks frequent use of a paper patch is more effective than tooth brushing for that reason that the paper patch can absorb pathogen, and can protect the oral mucosa barrier to prevent bacteria invasion of the blood circulation. Daily tooth brushing is the daily life habit of the people, by daily use of the paper patch (for middle aged and elderly people), the oral cavity can be cleaner, the heart can be healthier, and the brain can be more normal. The paper patch is a life prolonging health-care product for the middle aged and elderly people.
CN103360329A Phenazine compound and it application in preparation of anti-tumor drugs The invention discloses a phenazine compound and it application in preparation of anti-tumor drugs. The phenazine compound, i.e. a compound 1 or a compound 2 is a new compound, and the structural formula is shown as formula (I). The phenazine compound, i.e. the compound 1 or the compound 2 has an inhibiting effect on tumor cells, and can be used for preparing antitumor drugs to treat tumors. Therefore, a candidate compound for development of new anti-tumor drugs is provided by the invention, and has vital significance for development of Chinese marine drug resources. In the formula (I), for the compound 1, the R can be H; or for the compound 2, the R can be Me.
CN103393810A Medicament for treating bald tinea and preparation method thereof The invention discloses a medicament for treating bald tinea and a preparation method thereof. The medicament is mainly prepared from fructus evodiae, verdigris and croton seeds according to a certain weight ratio. The medicament has the functions of regulating the flow of qi, eliminating dampness, removing necrotic tissues and promoting wound healing, and is quick in response, good in curative effect and high in cure rate when used for treating bald tinea.
US7268122 Viricides; aids therapy The present invention relates to the use of N,O oversulfated K5 derivatives having a degree of sulfation higher than 3.2 or of their pharmaceutically acceptable salts for the preparation of pharmaceutical compositions for treating the infection and the consequent HIV/ADS disease.
CN102134268A Method for preparing panax japonicus saponin IVa and application of panax japonicus saponin IVa in preparing a medicament for protecting liver and lowering transaminase The invention discloses a method for preparing panax japonicus saponin IVa and an application of panax japonicus saponin IVa in preparing a medicament for protecting liver and lowering transaminase. The preparation method mainly comprises the following steps: crushing panax japonicus saponin IVa bulk pharmaceutical chemicals, extracting with water or a hydrophilic organic solvent, filtering and concentrating extract; passing the concentrated solution through a macroporous adsorption resin column chromatography column so as to enrich total saponin, eluting with water and an alcohol-water mixedliquid in turn, collecting the alcohol-water eluent, performing reduced pressure concentration at a low temperature, and drying to obtain the total saponin; and carrying out chromatograph separation on the total saponin, eluting with a solvent, recovering the solvent at reduced pressure, and drying so as to obtain crude panax japonicus saponin IVa; and repeatedly recrystallizing the crude productwith an organic solvent so as to obtain pure panax japonicus saponin IVa. According to verification, the panax japonicus saponin IVa has bioactivity of protecting liver and lowering transaminase, andcan be mixed with one or more of pharmaceutically acceptable carriers/auxiliary materials so as to be prepared into solid and liquid oral preparations with effects of protecting liver and lowering transaminase.
CN103030619A C-crystal-form 5-methyl-7-methoxyiso-flavone and preparation method, pharmaceutical compositions and application of C-crystal-form 5-methyl-7-methoxyiso-flavone The invention discloses a C-crystal-form 5-methyl-7-methoxyiso-flavone as well as a preparation method, pharmaceutical compositions and application of the C-crystal-form 5-methyl-7-methoxyiso-flavone. In particular, the invention discloses the C-crystal-form 5-methyl-7-methoxyiso-flavone at the solid state, the preparation method of a C-crystal-form sample, various preparations and pharmaceutical compositions prepared and developed by taking the 5-methyl-7-methoxyiso-flavone as an active ingredient, and the application of the preparations and pharmaceutical compositions for prevention of cardiovascular and cerebrovascular diseases, nervous system diseases, brittle-bone diseases, inflammation and metabolic diseases as well as in other disease medicines. The molecular structural formula of the 5-methyl-7-methoxyiso-flavone is shown in the specification.
CN102846706A Preparation process of integration-type novel formulation of Angelica sinensis blood enrichment decoction and production method thereof The invention relates to a preparation process of integration-type novel formulation of Angelica sinensis blood enrichment decoction and a production method thereof. The effective components of the novel formulation are made from the following raw materials (by weight parts): Angelica sinensis 30 and Astragalus membranaceus 6. The production method includes the steps of supersonic airstream pulverization, alcohol-water extraction, ultrasonic pulverization and extraction, water decoction and concentration, supersonic spray-drying, nano-scale grinding, high-pressure emulsion and homogenization and nanoparticle preparation. The production method integrates the advantageous of the nano-carrier combination technique, such as multi-component synergism and multi-target. The large-scale production can greatly reduce the production cost, greatly improve the product quality and enhance the target property and sustained/controlled-release property of drugs. The novel formulation is administered by oral intake and external application during four time periods respectively based on the midnight-noon tidal flow and human qi-blood flow rule. The novel formulation is also processed to membranes and transdermal delivery agents which are applied to different parts of human body respectively according to the midnight-noon tidal flow and human qi-blood flow rule and can be directly absorbed by the skin.
US20080207535 Polytetrafluoroethylene (PTFE), polyoxyethylene glycol (PEG), maleic anhydride (MA), and penicillin (ampicillin or gentamicin) are reacted to yield penicillin-PEG-MA-PTFE, which inhibits Grampositive bacteria Polymers are disclosed that are chemically modified to retard bacterial growth. Such modified polymers (e.g. ePTFE and polypropylene) are produced by first creating acid groups on the polymer surface through reactions with an anhydride. The acid groups are then linked to polyethylene glycol (PEG) through esterification or other reactions such as amidation. Preferably, at least two different molecular weight PEG species are employed. The antimicrobial surface is completed by linking antibiotics (e.g. β-lactam antibiotics) to the PEG extensions. One preferred embodiment of such a modified polymer is produced using ePTFE, maleic anhydride (MA), and penicillin (PEN) to yield PEN-PEG-MA-ePTFE, which inhibits gram-positive bacteria. The PEG spacer is critical for PEN function in this context, since PEN-ePTFE is ineffective against bacterial growth. Another preferred embodiment incorporates ampicillin (AMP) and a heterobifunctional PEG, HOOC—(CH2—CH2—O)n—NH2, to yield AMP-PEG-MA-ePTFE. This latter example inhibits both gram-negative and gram-positive bacteria.
EP1797889A1 Activated carbon for medical use Use of an activated carbon particles (I), preferably in the form of granules and pellets, for the production of medicaments, where the used activated carbon exhibits a large micro porous volume portion, related to the total porous volume of the activated carbon. An independent claim is included for a pharmaceutical composition comprising (I). - ACTIVITY : Antiinflammatory; Gastrointestinal-Gen. - MECHANISM OF ACTION : None given.
WO2008100618A3 Carbon-linked tetrahydro-pyrazolo-pyridine modulators of cathepsin s Carbon- linked tetrahydro-pyrazolo-pyridine compounds of formula (I) are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.
US20070015907 Repeat sequences of the ca125 gene and their use for diagnostic and therapeutic interventions The CA125 gene has been cloned and multiple repeat sequences as well as the carboxy terminus have been identified. The CA125 molecule comprises three major domains: an extracellular amino terminal domain (Domain 1); a large multiple repeat domain (Domain 2); and a carboxy terminal domain (Domain 3) which includes a transmembrane anchor with a short cytoplasmic domain. The amino terminal domain is assembled by combining five genomic exons, four very short amino terminal sequences and one extraordinarily large exon. This domain is dominated by its capacity for O-glycosylation and its resultant richness in serine and threonine residues. Additionally, an amino terminal extension is present, which comprises four genomic exons. The amino acid composition of the amino terminal extension was found to be consistent with the amino acid composition of the amino terminal domain. The molecular structure is dominated by a repeat domain comprising 156 amino acid repeat units, which encompass the epitope binding sites. More than 60 repeat units have been identified, sequenced, and contiguously placed in the CA125 domain structure. The repeat units encompass an interactive disulfide bridged C-enclosure and the site of OC125 and M11 binding. The repeat sequences demonstrated 70-85% homology to each other. Expression of the repeats was demonstrated in E. coli. The CA125 molecule is anchored at its carboxy terminal through a transmembrane domain and a short cytoplasmic tail. The carboxy terminal also contains a proteolytic cleavage site approximately 50 amino acids upstream from the transmembrane domain, which allows for proteolytic cleavage and release of the CA125 molecule. Any one of the repeat domains has the potential for use as a new gold standard for detecting and monitoring the presence of the CA125 antigen. Further, the repeat domains or other domains, especially the c-terminal to the repeat domain also provide a basis for the development of a vaccine, which would be useful for the treatment of ovarian cancer and other carcinomas where CA125 is elevated.
CN101732278A Coating technology of chlorophyll copper sodium tablet film The invention relates to the coating technology of a chlorophyll copper sodium tablet film, which is characterized in that the coating technique process of a film coat comprises the following steps of: properly and completely dissolving medicinal film coating powder to prepare 15 percent coating mixed suspension liquid to keep the temperature and store; placing a white tablet into a film coating pot at 40-50 DEG C; operating according to an operation program and setting a rotation speed to be 8-10rpm; starting a peristaltic pump when the white tablet is slightly heated; and adjusting the position of an adjusting spraying gun with a spraying speed of 5-8ml/min. The drying is carried out layer by layer, the surface color of the tablet is uniform and the tablet is discharged after blowing the cold air for 15-20 minutes. The tablet appearance quality, the weight difference, the disintegration time limitation and the like accord with quality standard requirement, thereby the coating time and the coating materials are saved.
CN102884049A Heterocyclic amides as ROCK inhibitors The present invention relates to new kinase inhibitors of formula (I), more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
EP2687509A2 Dicarboxyimides derivatives for use in the treatment of cancer The subject of the invention covers the substituted derivatives of dicarboximides represented by the general formula 1: possibly in the form of pharmaceutically acceptable salts, wherein R means the alkyl group C1-C6, optionally, the alkyl group is substituted with -OH group or amine group, selected from group containing -NH-R1 group or the group with formula 2 or 3, where R1, R2, R3 are the same or different and cover the alkyl group C1-C3 and R4 means -CH2- or -O- and the application of these compounds, or in combination with other drugs.
US20120009187 Cloning and recombinant productions of vespula venom protease and methods of use thereof The invention relates to nucleic acids encoding a novel Vespula venom protease or fragments thereof, in particular the protease Ves v 4, recombinant vectors comprising such nucleic acids, and host cells containing the recombinant vectors. The invention is further directed to the expression of such nucleic acids to produce a recombinant Vespula venom protease, or recombinant fragments thereof, or synthetic peptides thereof. Such a protease or fragments thereof or synthetic peptides thereof are useful for diagnosis of insect venom allergy and for therapeutic treatment of insect venom allergy.
US7064215 Nitrogen compounds such as 3-(5-morpholin-4-yl-1H-benz-imidazol-2-yl)-1H-indazole and/or isomers, used as immunology modulators, antidiabetic agents, antiogenesis inhibitors or for prophylaxis of Alzheimer's disease Organic compounds having the structure I are provided where the variables have the values described herein. Pharmaceutical formulations and medicaments include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compound or a pharmaceutically acceptable salt of the organic compound with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation or medicament according to the invention to a patient in need thereof.
US20120064060 Compound having s1p receptor binding potency and use thereof Provided are: a compound represented by formula (I): (wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocylic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, and when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt, an N-oxide form, a solvate, or a prodrug thereof; and a medicament which includes those. The compound of formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.
US20110223214 Use of carboxymethylcellulose to control ejectability and solidification time of compositions comprising one or more bioresorbable ceramics Carboxymethylcellulose, notably sodium carboxymethylcellulose or other alkali metal or alkaline earth metal salts of carboxymethylcellulose, are employed to control solidification time of compositions comprising one or more bioresorbable ceramics, notably a hydratable calcium sulphate, in order to facilitate preparation of a ready-to-use composition for inserting into the body by injection.
US7745427 (Calcitonin gene related peptide); azepinone ligands; 1-[(2-methoxyethyl)-2-oxo-6-phenylazepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide; analgesic, antiinflammatory agent; migranes, arthritis, neurodegenerative diseases The present invention is directed to compounds of Formula (I) and Formula (II) (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
CN102258788B Targeted transmission assembly of adriamycin anticancer medicine and preparation method thereof The invention discloses a targeted transmission assembly of an adriamycin anticancer medicine. The targeted transmission assembly is a ternary supermolecular assembly synthesized by using graphene oxide, folic acid modified cyclodextrin compound and adamantine modified porphyrin compound. The preparation method comprises: synthesizing folic acid modified beta-cyclodextrin and adamantine modified porphyrin respectively, absorbing the folic acid modified beta-cyclodextrin onto the graphene oxide under pi-pi action by using porphyrin as a medium, introducing folic acid onto the surface of graphene by using the strong noncovalent action of the adamantine and beta-cyclodextrin, and preparing the assembly by using the surface of the graphene oxide as the carrier of the pi-system adriamycin anticancer medicine. The invention has the advantages that: the synthesis route of the targeted medicine transmission assembly is simple, the yield of the targeted medicine transmission assembly is high, and the targeted medicine transmission assembly is suitable for amplified synthesis and use in actual production; and the assembly 1/2/DOX/GO is brought into a targeted cancer cell under endocytosis with a folic acid receptor in a malignant cell as a medium, so that the protection of normal cells and the targeted selective killing of cancer cells are realized.
US20100056499 3-amino-1-arylpropyl azaindoles and uses thereof The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
WO2005016942A1 Organophosphoric 4-iminohydantoin derivatives The invention relates to novel organophosporic 4-iminohydantoin derivatives of general formula (I) and above all the use thereof as a pharmaceutical or herbicidal agent.
US20130071323 Therapies for hematologic malignancies The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administering a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R′ is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable excipient; and administering at least one additional therapeutic agent.
US20120178816 Carbamide peroxide treatments for the reproductive tract Disclosed are methods of maintaining fertility or treating retained placenta, reproductive tract infection, or reproductive tract inflammation in an animal by administering carbamide peroxide to the reproductive tract of the animal. The carbamide peroxide administration removes placental remains on the uterine wall, protects against or treats reproductive tract infection, and protects against or treats reproductive tract inflammation such as metritis, and thereby maintains fertility in the animal.
CN101219140B Benzydamine Hcl soluble tablet and method for preparing the same The invention provides a benzydamine hydrochloride soluble tablet, which is characterized in that: the benzydamine hydrochloride soluble tablet comprises effective dose of benzydamine hydrochloride and a filling agent, a disintegrating agent, a lubricant and a wetting agent in right amounts. The product of the invention used for the treatment of bacterial vaginosis has the effects of quick dissolution, quick release, high efficiency and safety. A preparation method of the benzydamine hydrochloride soluble tablet is also provided in the invention.
WO2014068527A1 Bruton's tyrosine kinase inhibitors Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I)
US20100069421 Compositions and methods for the treatment of radiation proctosigmoitis The present invention provides a new method of preventing, ameliorating and/or treating enteritis induced by abdominopelvic therapies. The present invention also relates to the prophylactic treatment of traveler's diarrhea.
CN103054168A Lotus incense type snuff The invention belongs to the technical field of snuff products, relates to lotus incense type snuff made of pure natural raw materials and further relates to a preparation method of the snuff. The snuff comprises the pure natural raw materials of, by weight, 50-150 parts of biond magnolia flower, 10-90 parts of rhizoma atractylodis, 100-300 parts of herba eupatorii, 0.1-0.4 part of borneol, 0.03-0.10 part of asarum, 0.01-0.09 part of rhinoceros horn, 5-15 parts of curcuma, 25-125 parts of tobacco leaves, 2-6 parts of agilawood, 2-6 parts of cloves, 5-25 parts of angelica root, 2-6 parts of menthol, 0.05-0.35 part of musk, 100-500 parts of green tea leaves and 50-150 parts of red wine. The snuff is fumigated by lotuses, thereby having lotus incense. The snuff is capable of energizing and refreshing, enabling the nasal cavity to be ventilated and assisting in smoking cessation. The snuff has fresh and elegant lotus incense after being fumigated by the lotuses, thereby being capable of relaxing, enhancing memory, energizing, refreshing and making people feel hopeful.
US20110082203 Process to diagnose or treat brain injury A process for diagnosing and treating a neurological condition in a subject is provided that includes assaying a biological sample of a subject for the presence of one or more biomarkers; diagnosing a neurological condition based on a ratio of one or more of the biomarkers in the sample; and administering a therapeutic to the subject to alter the ratio of one or more biomarkers. The diagnosis numerous neurological conditions such as brain injury, or multiple organ injury is provided.
US7169925 Indole derivatives as interleukin-4 gene expression inhibitors This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.
CN103724281A Novel derivative of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propyl and application of novel derivative The invention discloses a novel derivative of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propyl and application of the novel derivative. The novel derivative has good medicine activity, can greatly prolong the half-life period of a medicine, prolongs the retention time of the medicine in a human body, and meanwhile, improves the concentration of the medicine in blood; therefore, a better curative effect is achieved. As the half-life period of the medicine is greatly prolonged, activity concentration of the medicine in the blood can be maintained for a longer period of time; under the cure condition of dose constrain, the curative effect is maintained and the dosage of the medicine is reduced, so that the problem of bad metabolism of the medicine is eliminated, the medicine toxicity is reduced, and the toxic and side effects in the medicine use process are reduced.
CN103520143A Nerve protective composition and application thereof The invention discloses a nerve protective composition, comprising sesamin derivatives, and food or pharmaceutically acceptable supporting agent or excipient, wherein the sesamin derivatives have the chemical structural formula shown in the specification, and in the chemical structural formula, R<1> and R<2> are independently selected from hydroxyl, (C1-C6) alkyl, (C1-C6) alkoxy, O-(C1-6) alkyl and CORc, and R<3> and R<4> are independently selected from hydroxyl, (C1-6) alkyl and (C1-6) alkoxy. The nerve protective composition disclosed by the invention can be applied to prevention of nerve damage, for example, prevention of nerve cell damage caused by epilepsia or abnormal accumulation of amyloid beta protein (Abeta).
WO2012028311A1 Compositions comprising a taxane for coating medical devices The present invention relates a pharmaceutical composition comprising a taxane and an inhibitory compound capable of inhibiting the enzyme acetaldehyde dehydrogenase e.g. disulfiram. The pharmaceutical compositions of the invention can be used to coat medical devices such as implants. Such implant can be an expansible hollow part, having at least one opening, which consists of an elastic biocompatible material that comprises elongated micro - cavities in its surface. Medical devices coated with a pharmaceutical composition of the invention exhibit an enhanced transfer of taxane from the surface of said medical device into the target tissue.
WO2014009295A1 Imidazopyridine derivatives as modulators of tnf activity A series of imidazo[l,2-a]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
EP2270006A1 Pyridazine derivatives useful as vanilloid receptor ligands Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders. or any pharmaceutically-acceptable salt thereof, wherein: J is O or S; X is = C(R2); Y is N;
EP1299374B1 Novel non-psychotropic cannabinoids Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or inflammatory disorders comprising as active ingredient the stereospecific (+) enantiomer, having (3S, 4S) configuration of Δ6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to acute injuries to the central nervous system, including mechanical trauma, compromised or reduced blood supply as may occur in cardiac arrest or stroke, or poisonings. They are also effective in the treatment of certain inflammatory disorders and chronic degenerative diseases characterized by neuronal loss and chronic pain including neuropathic pain.
CN101732421A Method for preparing total flavonoids, total tannins and galic acid compounds of polygonum capitatum The invention relates to a method for preparing total flavonoids, total tannins and galic acid compounds of polygonum capitatum. The method comprises the following steps: quenching polygonum capitatum by 40 to 80 percent ethanol (methanol or acetone) or coating refluxed extract on D101 macroporous resin, eluting the polygonum capitatum by 70 to 85 percent ethanol (or methanol), coating concentrated eluant on an MCI column, eluting the MCI column by water, performing water solution and alcohol precipitation after concentrating the eluant, and obtaining the galic acid compounds when concentrating supernatant liquid to extractum; eluting the galic acid compounds by 80 percent ethanol (or 85 percent methanol), concentrating the eluant to extractum, after dissolving the extractum by 95 percent ethanol, coating the solution on a SephadexLH-20 gel column, eluting the gel column by 95 percent ethanol to colorlessness, and obtaining the total flavonoids when concentrating the eluant to extractum; and eluting residue on the column by 50 to 100 percent acetone to colorlessness, and obtaining the total tannins when concentrating the eluant to extractum.
CN101933928A Method for preparing medicament for treating chicken colibacillosis The invention discloses a method for preparing a veterinary medicament, in particular a method for preparing a medicament for treating chicken colibacillosis. The method for preparing the medicament for treating the chicken colibacillosis is characterized by comprising the following steps of: dissolving gelatin into water, putting glycerol into the water to obtain gelatin size, and adding p-hydroxy benzoic acid ethyl ester ethanol solution into the gelatin size to form composite solution after mixing; and dissolving enrofloxacin soluble powder into the water to obtain suspension, putting the composite solution into the suspension, adding formaldehyde solution into the solution for curing, and drying the cured product in vacuum to obtain the medicament. The prepared medicament for treating the chicken colibacillosis is used for treating the chicken colibacillosis; the enrofloxacin soluble powder dispersoid serving as a core is wrapped by a high-quality macromolecular material and cured to obtain the medicament, so the palatability of the enrofloxacin and the affinity in the body are improved, the duration of the blood concentration peak of the enrofloxacin is longer and the action is more durable.
WO2005051317A2 Substituted imidazo ring systems and methods Imidazo ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
US7157240 MID 4460, a human tyrosine phosphatase family member and uses therefor The invention provides isolated nucleic acids molecules, designated MID 4460 nucleic acid molecules, which encode novel tyrosine phosphatase family members. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing MID 4460 nucleic acid molecules, host cells into which the expression vectors have been introduced, and nonhuman transgenic animals in which a MID 4460 gene has been introduced or disrupted. The invention still further provides isolated MID 4460 proteins, fusion proteins, antigenic peptides and anti-MID 4460 antibodies. Diagnostic and therapeutic methods utilizing compositions of the invention are also provided.
US20110280809 Pdia4, target of cytopiloyne derivatives, for tumor diagnosis and treatment Methods of diagnosing cancer that are based in part on the findings that Pdia4 promotes cell growth, cell proliferation, and cell cycle are disclosed herein. Methods of using microvessel density as a surrogate marker and reducing tumor microvessel density in a subject are also enclosed herein.
US20110144214 Hydroalcoholic gel compositions for use with dispensers A hydroalcoholic gel composition includes greater than about 40 weight percent of an alcohol, based upon the total weight of the alcoholic composition, a polyacrylate thickener, and an ester plug-preventing agent. The composition is suitable for use in dispensers, and exhibits reduced mis-directed output when the dispenser is actuated.
US7026337 Gel formulations of hydroxypyridone derivatives, which contain solvents and hydrophilic gel-forming agents make possible a high release of the active compound A pharmaceutical preparation comprising a hydrophilic gel-forming agent, water and a compound of the formula I is suitable for the treatment and prophylaxis of dermatomycoses.
CN102040558A Substituted bicyclo(3,3,1)nonane ether compound and application thereof The invention relates to a substituted bicyclo(3,3,1)nonane ether compound and application thereof. The compound comprises an optical isomer, quaternary ammonium salt and medicinal compositions thereof. The compound can be used for treating diseases or symptoms which are associated with a central nervous system, a peripheral nervous system, smooth muscle contraction, endocrine, neurodegeneration, inflammation, pain, withdrawal symptoms caused by termination of abuse of chemical substances and the like.
CN103113350A Novel crystal form of R-rabeprazole sodium hydrate, preparation method and application thereof The invention discloses a novel crystal form of an R-rabeprazole sodium hydrate. The characteristic peaks of powder, shown in the form of diffraction angles 2theta in an X-ray diffraction diagram, are respectively 6.986, 9.009, 9.667, 13.398, 13.954, 14.473, 17.077, 18.021, 19.439, 22.880, 27.007, 31.496 and 32.525+/-0.2. The crystal form is good in stability. The invention also provides a preparation method and application of the crystal form. The preparation method for preparing the novel crystal form of the R-rabeprazole sodium hydrate has the characteristics of being high in repeatability and high in operability; and the preparation method can be carried out to prepare a medicine composition for treating the diseases caused by hyperacidity.
WO2011084652A3 Crystalline salts of a factor xa inhibitor The present invention provides salts and crystalline forms of the compound 5-chloro-N-((1-(4-(2-oxopyridin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide, and pharmaceutical compositions and method of use thereof.
CN103211800A Patch used for treating nausea and vomiting, and preparation method thereof The invention relates to a transdermal patch used for treating nausea and vomiting, and a preparation method thereof. The invention provides a transdermic-absorption frame-work patch. A ransdermic-absorption preparation layer composed of an acrylic adhesive, isopropyl myristate, diethanolamine laurate, rosin ester, and granisetron with a weight ratio of 40-70:5-30:2-10:5-24:5-15 is laminated on one side of a backing layer which is non-permeable to medicine.
WO2014100359A1 Novel ergoline derivatives and uses thereof Provided herein are 8'-Hydroxy-2-CF3-dihydroergotamine (8 ' OH-2-CF3 -DHE) compounds, compositions, and dosage forms containing such compositions. Also provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.
CN101991598A Use of sulfated fucan in preparing medicines for treatment of gastrointestinal diseases The invention relates to a new pharmaceutical use of sulfated fucan, more particularly to a use of sulfated fucan in preparing medicines for the treatment of gastrointestinal diseases. Gastric diseases include gastritis, gastric ulcer, doudenal ulcer, enteritis or colitis. The gastritis include a variety of acute and chronic gastritises such as superficial gastritis, hypertrophic gastritis and the like. The main pharmacodynamics tests of sulfated fucan as gastrointestinal diseases show that sulfated fucan includes particular protective effect for both gastric ulcer induced by ethanol in mice and reserpine gastric ulcer. The preliminary statistics on the clinical treatment results of 50 different patients with gastric disease represents that, 22% of the patients are cured after the administration of sulfated fucan, 40% is effective, 22% is excellent, 16% is ineffective and the total effective rate is 84%, thus the sulfated fucan can obtain remarkable curative effect, has no toxic and side effect and is safe and reliable.
WO2014160689A1 Piperazine and homopiperazine derivatives as hiv attachment inhibitors Compounds of Formula I, including pharmaceutically acceptable salts thereof, are useful as HIV attachment inhibitors.
EP1453492B1 Use of quinazolines to treat t-cell mediated diseases The invention concerns the use of the quinazoline derivatives of Formula (I) Wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions such as autoimmune diseases like transplant rejection or rheumatoid arthritis in a warm-blooded animal.
US20110217372 Fast dissolving oral tablets and method for production thereof Provided is a fast dissolving oral tablet, and a method for the production thereof, including the steps of: compressing a mixture of active ingredients, pharmaceutically acceptable additives, and supercritical fluid-soluble substances to produce the tablets; and allowing the tablets to contact a supercritical fluid to extract supercritical fluid-soluble substances from fine pores in the tablets.
US20110178042 Hydroxamic Acid Derivatives Useful as Antibacterial Agents The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
US20090176738 Dermal medicament delivery system There is provided a means of applying a heated medicament to the skin and concurrently hydrating the skin thus raising the efficacy of administration.
CN101966171B Hydrosoluble reduced enzyme Q10 composition and preparation method thereof The invention relates to a hydrosoluble reduced enzyme Q10 composition and a preparation method thereof, and provides a hydrosoluble reduced enzyme Q10 composition, which comprises raw materials and following mass components thereof: a reduced enzyme Q105-15, a hydrosoluble carrier 10-120, and an emulsifier 0.5-40; wherein the hydrosoluble carrier is one or more of maltose, CMC, gum rubber, soluble starch, lactose, fructose, sorbierite, mannitol, acacia and carrageenan; and the emulsifier is nonionic surfactant. The invention further provides the preparation method of the hydrosoluble reducedenzyme Q10 composition. In the method, the indissoluble reduced enzyme Q10 is mixed with the hydrosoluble carrier and the emulsifier to prepare the hydrosoluble reduced enzyme Q10 composition, advantages of an inclusion technology and a solid dispersion technology are synthesized, defects in the technologies are solved, a problem of slightly solubility of the reduced enzyme Q10 is solved, a series of tests shows that the reduced enzyme Q10 has water-solubility, high solubility, high dissolution rate, high stability and high active substance content.
CN103211804A Applications of acetate in preparation of medicines for improving diabetes The invention discloses applications of acetate in preparation of medicines for improving diabetes. Results of experiments about of a small-dosage multi-time streptozotocin injection initiated diabetic mouse model show that acetate can substantially inhibit the mouse random blood sugar rise caused by MLDS, substantially improve the mouse sugar tolerance abnormity caused by the MLDS, substantially improve the content of insulin in the mouse serum processed through the MLDS, and substantially inhibit the MLDS caused expression of inflammatory factors in the mouse spleen. An evidence that acetate can be used for treating MLDS induced diabetes of animal models is provided in the invention for the first time, and it is prompted that acetate may have a certain improvement effect on diabetes clinically.
CN103446059A Pharmaceutical composition of cefonicid sodium for injection and lidocaine hydrochloride injection The invention relates to a pharmaceutical composition of cefonicid sodium for injection and 1% idocaine hydrochloride injection, and in particular relates to a combined application package, comprising cefonicid sodium for injection and 1% lidocaine hydrochloride injection. When in a use, the cefonicid sodium is dissolved fully into the 1% lidocaine hydrochloride solution. The pharmaceutical composition not only has broad-spectrum antibacterial function but also can remarkably reduce local pain caused by the injection of cefonicid sodium.
CA2840354A1 Novel formulations and methods for treating dermatological disorders or diseases The present invention provides compositions and methods for treating a dermatological disorder or disease.
EP1589000A2 (R)-Chiral halogenated 1-substitutedamino-(N+1)-alkanols useful for inhibiting cholesteryl ester transfer protein activity The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
US20090123534 comprising progesterone, soy bean lecithin, and olive oil, wherein at least about 80% of the particles of progesterone are characterized by a particle size of between 1 and 15 mu m; for treating a physiological condition linked to insufficiency of progesterone secretion The present invention relates to a pharmaceutical composition comprising micronized progesterone, soya bean lecithin, and at least one oil selected from the group consisting of sunflower oil, olive oil, sesame seed oil, colza oil, almond oil, to the method for the preparation thereof and to the uses thereof for treating a physiological condition linked to insufficiency of progesterone secretion.
CN103417533A Application of TPCA-1 as STAT3 signal inhibitor in preparation of antitumor drug The invention provides a new medical application of TPCA-1 which serves as an STAT3 signal inhibitor to be used in preparation of an antitumor drug. Cell model screening experiments and Western-Blot detection experiments prove that TPCA-1 has excellent inhibitory activity and can effectively inhibit the expression of relevant gene which is regulated by STAT3, so as to effectively inhibit the growth of a tumor cell which is needed by the STAT3 signal. Therefore, TPCA-1 is taken as the major active ingredient, technology and accessory which are acceptable in pharmaceutics are adopted for the preparation of antitumor drug taking STAT3 as a target in various dosage forms, and a promising development prospect can be predicted.
US20120309818 Chronic inflammation and transplantation Embodiments of the present invention feature methods for treating inflammatory disease and transplantation characterized in that it includes: (i) the incubation of organs with one or more Bryostatin-1 derivatives under conditions which permits vascular exposure to these compounds prior to or immediately following organ ‘harvesting’, and (ii) intravenous, transdermal, intraperitoneal, intra-alveolar instillation of Bryostatin-1 in vivo during active disease, or during periods of disease remission and (iii) prophylactic administration of Bryostatin-1 to limit the development of GVHD.
EP2400843A1 Iminosugars and methods of treating arenaviral infections Provided are methods of treating a disease or condition caused by or associated with a virus belonging to the Arenaviridae family using iminosugars, such as DNJ derivatives.
CN101129362A Sirolimus dispersible tablets and method of producing the same The invention relates to a cirolemycin dispersing tablet and the preparing method, which prepare medicine and immunosuppressant with cirolemycin as the main material. The preparing method comprises the following steps: dissolving cirolemycin, bo luo sha mu F68, hydroxypropyl betacyclodextrin and 1/2 micornizing silica gel with absolute ethyl alcohol; drying into the powder in the atmospheric temperature and decompression condition; mixing crystalline cellulose, cross bonding polyketone and 1/2 micornizing silica gel; drying; adding dolomol in the above powder; pelleting after mixing; getting the product. The cirolemycin dispersing tablet is continent to have, which has the good absorbability, the little gastrointestinal hormone, is fit for the old man and the dysphagia body, has the low loss in the total absorption process, has the good stability owing to adding the disintegration agent and bulk additive with the good disintegrability, can disintegrate quickly when meeting water, forms the uniform turbid liquor, and has the high bioavailability. The invention has the simple technology, which doesn't have the special requirement, and is fit for the mass production.
US20120108647 Therapeutic uses of inhibitors of rtp801l The present invention provides novel molecules, compositions, methods and uses for treating microvascular disorders, eye diseases respiratory conditions and hearing disorders based upon inhibition of the RTP801L gene and/or protein.
WO2008007149A2 New medical use of triazine derivatives Compounds of formula (I) especially where R1 is an optionally substituted alkyl, aralkyl or heterocyclyl-alkyl group, are shown to have activity as sodium channel blockers or as antifolates. Some novel compounds where R1 is an aralkyl or heterocyclyl-alkyl are disclosed.
WO2013162298A1 Novel beta-alanine derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical composition comprising same as active ingredient The present invention relates to novel beta-alanine derivatives, to the pharmaceutically acceptable salts thereof, and to a pharmaceutical composition comprising same as an active ingredient. The novel beta-alanine derivatives and pharmaceutically acceptable salts thereof according to the present invention may effectively inhibit the activity of DGAT1, which is an enzyme serving as a catalyst in the final step of the synthesis of neutral lipids, and therefore can be effectively used as a pharmaceutical composition for preventing or treating various diseases relating to lipid metabolism belonging to the group consisting of obesity, dyslipidemia, fatty liver, insulin resistance syndrome, and hepatitis.
CN103127115A Composition capable of curing abnormal blood lipid The invention relates to a composition capable of curing abnormal blood lipid. The composition capable of curing the abnormal blood lipid comprises ezetimibe, atorvastatin calcium and acipimox. The range of weight ratios of the ezetimibe, the atorvastatin calcium and the acipimox in the composition is 5-10: 5-80: 250-1000, preferably 10: 10-40: 250-750 and optimally, 10: 10-20; 500-750. The composition capable of curing the abnormal blood lipid is strong in blood lipid regulating effect, comprehensive in function and little in side effect.
CN101278898A Sustained-release injection containing aminoside antibiotics and uses thereof The invention relates to a slow-released injection comprising aminoglycoside antibiotic, which comprises a slow-released microsphere and a dissolvent; the slow-released microsphere comprises a slow-release adjuvant and the aminoglycoside antibiotic; the dissolvent is the special dissolvent which comprises a suspending agent such as sodium carboxymethylcellulose, etc., and the viscosity of which is 100cp-3000cp (at 20 DEG C-30 DEC C); the slow-release adjuvant can be selected from EVAc, polifeprosan, PLA, PLGA, sebacic acid copolymer, albumen glue and gelatin, etc.; the slow-released microsphere also can be made into a slow-released implant and an ointment. The slow-released implant and the slow-released injection can be partially placed or injected in a bacterial focus to release locally and slowly for more than 5-30 days, thereby obviously reducing the toxicity of the entire body while getting and maintaining a valid medicine density in the local focus effectively. The slow-released injection comprising the aminoglycoside antibiotic of the invention has obvious special treatment effect for focus of local infection such as chronic osteomyelitis, severe bedsore, refractory skin ulcer, diabetic foot, osteonecrosis of femoral head and various abscesses, etc., caused by staphylococcus, streptococcus, peptostreptococcus, propionibacterium acnes, enterobacter, tubercle bacillus, gonococcus and meningococcus, etc.
EP1284754B1 Gel-like pharmaceutical composition for subcutaneous administration comprising bisphosphonic acids or their salts The invention is concerned with a pharmaceutical preparation for subcutaneous, parenteral administration, which contains bisphosphonic acids or their salts as the active substance, as well as the production of this preparation. By means of the preparation in accordance with the invention it is possible to administer locally relatively high concentrations of bisphosphonates without the occurrence of incompatibilities.
CN102119921A Aivlosin injection for swine and preparation method thereof The invention relates to an aivlosin injection for swine. Each 100ml of tylosin injection contains 20g of acetylisovaleryl tylosin tartrate, 20-35g of propylene glycol, 10-15g of N,N-dimethyl acetamide, 2-4g of benzyl alcohol, 0.1-1.0g of di-tert-butyl-4-methylphenol and balance of glyceryl triacetate. The preparation method comprises the following steps of: mixing the glyceryl triacetate, the propylene glycol, the benzyl alcohol and the N,N-dimethyl acetamide evenly to obtain an oil phase; adding an antioxidant to the oil phase and stirring until the added particles are dissolved; and adding the aivlosin and stirring to dissolve. The aivlosin injection for swine adopts the oily solvent as a solvent, the medicament is dissolved in the oily solvent, and the elimination half life of the medicament in an animal body is prolonged by the characteristic of slow elimination of the oily solvent after intramuscular injection.
US20070128206 enhancing antigenicity of a vaccine by administering a sugar cane-derived extract having a low saccharide concentration obtained by column chromatography; ion exchange resin; A preventive or remedy for infection, an anti-endotoxin agents, a vaccine adjuvants and a growth promoter each comprising a sugar cane-derived extract as an active ingredient which agent is safe to man and animals. Also presented are foods and feeds comprising these agents.
US7291627 E.g., 8-chloro-3,11-dimethyl-5,6-dihydroimidazo[5,1-a]- beta -carboline methane sulfonate; used for reducing alertness and/or for accelerating the onset of sleep The invention concerns dihydroimidazo[5,1-a]-β-carboline compounds of general formula (I) wherein in particular, R1, R2, R3, R4, R6 and R7, identical or different, independently of one another, present a hydrogen, halogen atom, an alkyl, hydroxyl, alkoxy, trihalogenoalkyl, alkylamino, dialkylamino, aryl, arylalkyl, carboxy, alkylcarbonyloxy, acyl, aryloxy or arylalkoxy group; R5 represents a hydrogen atom, an alkyl or arylalkyl group; and their isomers as well as their addition salts to a pharmaceutically acceptable acid. The inventive compounds are for use in medicine, in particular as hypnotics.
CN103690573A Natural pharmaceutical composition for enhancing immunity and preparation method of natural pharmaceutical composition The invention discloses a natural pharmaceutical composition for enhancing immunity and a preparation method of the natural pharmaceutical composition. The composition is mainly prepared from the following raw materials in parts by weight: 95-185 parts of ganoderma spore extract, and 5-15 parts of lycopene. The pharmaceutical composition has the healthcare function of enhancing immunity; the curative effect is significantly improved when compared with that of a single medicinal material; the dose is obviously reduced when compared with that of the single medicinal material; the toxic and side effects of the natural pharmaceutical composition are reduced when compared with those of the single medicinal material.
CN101601677A Establishment and application of model for screening medicaments for resisting heterogeneous and multi-reason senile dementias The invention relates to the establishment of a model for screening medicaments for resisting heterogeneous and multi-reason senile dementias, which is characterized in that the common carotid arteries on two sides of each group of aging rats are ligated repeatedly to block blood flow, the rats are fed for three days after operations, and the alive rats in good condition are intracerebrally injected with Abeta1-40 (incubated 1 W at a temperature of 37 DEG C) which is diluted to be 5 micrograms per microliter by sterile normal saline. The establishment has the following advantages: by using the model, a damage model of the aging rats with declined learning and memory functions is provided for the studies on the nosogenesis of old age AD, VD and mixed dementias and the correlative curative effect of medicaments, and the model can reflect the actual brain pathology damage conditions of senile dementia patients.
US20120277292 ANTISENSE OLIGONUCLEOTIDES AGAINST cPLA2, COMPOSITIONS AND USES THEREOF Antisense oligonucleotides against cPLA2 are provided, which are capable of inhibiting cPLA2 expression as well as superoxide production, especially in phagocytes. These antisense oligonucleotides are powerful agents for the treatment of inflammatory conditions, in particular arthritis, as well as in neurodegenerative diseases. The antisense oligonucleotides or compositions comprising the same may be used in methods of treatment of such diseases.
WO2007019867A1 Novel 2,3-dihydroindole compounds The invention relates to compounds of the formula I, wherein the variables are as defined in the claims. The compounds are useful in the treatment of a disease where a D4 receptor and/or a 5-HT2A receptor is implicated.
CN103127084A Application of Aphanamixoid A to platelet increasing medicine The invention relates to novel application of a compound, namely Aphanamixoid A, to the field of pharmacy, in particular to application of the Aphanamixoid A to preparation of platelet increasing medicine. The application of the Aphanamixoid A to the preparation of the platelet insufficiency treatment medicine is made public for the first time. The skeleton type is fully novel, activity of the Aphanamixoid A in treating platelet insufficiency is surprisingly strong, the possibility that inspiration is obtained from other compounds does not exist, and therefore the Aphanamixoid A has prominent substantive features, and meanwhile, significant progress of the application of the Aphanamixoid A to prevention and treatment of the platelet insufficiency is obviously achieved.
EP2729454A1 Novel trifluoromethyl-oxadiazole derivatives and their use in the treatment of disease The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.
EP1409480B1 Pyrrolo-indole and pyrrolo-quinoline derivatives as prodrugs for tumour treatment Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 and optionally also R3 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumours. The prodrug is expected to be activated preferentially in tumour cells, where it will act as a DNA alkylating agent preventing cell division.
CN103599098A Composition of compatibility of curcumin and bilobalide B, and application of composition The invention discloses a composition of compatibility of curcumin and bilobalide B, and an application of the composition, and belongs to the field of medicines. The composition of compatibility of the curcumin and the bilobalide is prepared from the following medicinal materials in parts by weight: 1-8 parts of curcumin and 1 part of bilobalide B in a manner of evenly mixing. The pharmaceutical composition has a synergistic effect on treatment of a polycystic kidney disease, and is superior to single medication.
CN101897670A Azithromycin enteric-coated pellet capsule and preparation method thereof The invention relates to an azithromycin enteric-coated pellet capsule and a preparation method thereof. The capsule comprises azithromycin mixed preparation auxiliary material which is loaded into a pellet core to form a pellet pill that is covered by isolation coating material to form an isolation layer and covered by enteric-coated material to form an enteric-coated layer. The invention azithromycin enteric-coated pellet capsule solves the problems in the background technology, can be dissolved and absorbed in intestinal tract, is rapidly and evenly dispersed in the intestinal tract after entering into the intestinal tract, and effectively improves the bioavailability of medicine. The invention also provides the preparation method of the azithromycin enteric-coated pellet capsule.
EP1790345A1 Triazin beta-secretase inhibitors It has been found that compounds of formula (I) wherein, in preferred embodiments X1 and X2 are N-H or N-R3 or N-R4, RN and RC are both H R1 and R3 are independently from each other optionally substituted phenyl, or R1 and R2 and/or R3 and R4 form together with the N to which R2 and/or R4, respectively, are bound a 5 or 6 membered heterocycle comprising 1 or 2 heteroatoms, and A is preferably halogen substituted phenyl or a preferably phenyl substituted furanyl are good β-secretase inhibitors for the treatment of Alzheimer's disease.
CN102342977A Keteling capsule and preparation method thereof The invention discloses a Keteling capsule and a preparation method thereof. The Keteling capsule consists of ficus microcarpa and chlorphenamine maleate. The Keteling capsule disclosed by the invention is mainly used for treating chronic bronchitis and is a new medicament for relieving a cough. The Keteling capsule is used for relieving various cough symptoms such as acute and chronic bronchitis, bronchial asthma, cough caused by cold, whooping cough and the like, eliminating phlegm, relieving asthma and diminishing inflammation and is also used for relieving cough with dyspnea and cough caused by chronic bronchitis.
EP1120409B1 2,3-disubstituted pyridine derivatives, process for the preparation thereof, drug compositions containing the same and intermediates for the preparation Compounds represented by general formula (I) (wherein A is O, S, CHR?1 or NR2; R1 and R2¿ are each H or lower alkyl; X?1 and X2¿ are each H, halogeno, nitro, cyano or the like; Y1 is H or lower alkyl; Z?1 and Z2¿ are each H, halogeno, cyano, hydroxy, lower alkyl or the like; and n is an integer of 2 to 4), and physiologically acceptable salts thereof; a process for the preparation of both; drug compositions containing the same as the active ingredient; and intermediates for the preparation. The compounds (I) exhibit potent PDE IV inhibiting and excellent bronchodilating activities, and are therefore useful as PDE IV inhibitors and as therapeutic and preventive drugs for various allergic inflammatory diseases, organ inflammatory diseases and so on, particularly airway-obstructive lung diseases including asthma.
CN1679543A Medicine containing active components of methylcantharidimide and its preparing method and use An injection containing methylcantharidimide for treating primary liver cancer and chronic viral hepatitis B is prepared through dissolving methylcantharidimide in solvent, decarbonizing, filtering, freeze drying and sterilizing.
CN102911040A Sesquiterpenoids from marine fungi source as well as preparation method and application thereof The invention discloses sesquiterpenoids from a marine fungi source as well as a preparation method and an application thereof. The structural formula of the sesquiterpenoids is shown as a formula (I). The sesquiterpenoids have activity for inhibiting tyrosine phosphatase (mPtpB) and acetylcholinesterase (AchE) and can be used for preparing medicines resistant to tuberculosis and senile dementia. The formula (I) is described in the specification.
CA2391239C Benzopyran derivative and antiallergic agent The present invention provides a compound which is highly safe in terms of toxicity and has a stronger antiallergic action, and particularly has an action of inhibiting both immediate and delayed type allergic reactions. A benzopyran derivative represented by the general formula (I): wherein R1 is an alkyl group having 1-10 carbon atoms or an alkenyl group having 2-10 carbon atoms, and one of R2, R3, R4, and R5 is an alkoxy group substituted with a hydroxygroup or an alkoxy group substituted with a carboxy group, and the others are hydrogen atoms or physiologically acceptable salts thereof are superior as the active ingredient of an antiallergic agent.
WO2008067774A1 An antimycotic pharmaceutical composition An antimycotic pharmaceutical composition comprising the 2-aminothiazoles of the general formula (I) and corticoid drugs and the use of which for the treatment or prevention skin infection caused by fungus, wherein the definition of substituent group of general formula (I) as described in the description. Particularly, the antimycotic pharmaceutical composition can be used to treat or prevent skin infection caused by fungus, superficial fungal diseases, itching, the mixed infection caused by fungus and bacterium or various dermatitis
CN103172618A Ilaprazole crystal form and preparation method thereof The invention discloses an ilaprazole crystal form X and a preparation method thereof. The ilaprazole crystal form X disclosed by the invention is easy to prepare. The ilaprazole crystal form X provided by the invention is high in purity and low in impurity content. The preparation method disclosed by the invention is low in required solvent amount and low in production cost. The preparation method is simple to operate, mild in reaction conditions, easy to control, and can obtain a target product crystal form in an extremely determined and good-reproducibility mode.
US20120207825 Pharmaceutical compositions for reducing alcohol-induced dose dumping A pharmaceutical composition is disclosed. The composition comprises a core comprising an active substance or a salt thereof; a separating layer comprising at least one sugar; and a functional layer comprising at least one pharmaceutically acceptable polymer, wherein the composition is resistant to dose dumping in presence of alcohol.
CN102949405A Application of tea saponin and preparation thereof The invention discloses an application of tea saponin used as a malassezia inhibitor, and in particular relates to an application for preparing drugs for treating skin diseases caused by malassezia. The invention further discloses an external preparation and daily cosmetics containing the tea saponin.
WO2011030106A1 Cancer cell apoptosis There is described a therapeutic agent capable of directly or indirectly having an effect on the proteins N-methyl-D-aspartate (NMDA), Cyclooxygenase-2 (COX-2), Tumour Necrosis factor alpha (TNF-a), Nuclear factor-kappa B (NFKB), Cyclin- dependent kinases, e.g. CDK2/A and CDK5/p25, Histone acetyltransferase (HAT) and Farnesyltransferase, simultaneously, sequentially or separately. There is especially described dexanabinol, or a derivative thereof, as the therapeutic agent.
US20090118211 Compositions and Methods for Enhancement of Sexual Function Novel compositions and methods which utilize an erection-enhancing agent and an ejaculation-delaying agent, such that these agents provide an overlapping and/or synergistic effect, are provided. These composition and methods can be beneficially utilized for treating sexual dysfunction and/or for enhancing sexual function.
EP2774611A1 Magnetic composition, and method for producing same A magnetic composition containing a metal-salen complex compound which can be securely guided by a magnetic field to a target area to be preferably treated, and a method for producing the magnetic composition are provided. The magnetic composition is prepared by dispersing magnetic particles, which are obtained by coating a metal-salen complex compound with a dispersant, in a polar solvent by means of the dispersant. Furthermore, the magnetic composition production method includes a first step of mixing the metal-salen complex compound with the dispersant in an organic solvent and coating the metal-salen complex compound with the dispersant and a second step of dispersing the metal-salen complex in a polar solvent.
CN102058487A High-point indication paste of denture base and preparation method thereof The invention discloses a high-point indication paste of a denture base, comprising the basic components in percentage by weight: 50-60 percent of zinc oxide, 10-20 percent of talcum powder, 15-25 percent of Vaseline and 2.5-7.5 percent of edible sesame oil. The preparation method of the high-point indication paste comprises the following steps of: respectively and finely grinding the zinc oxide and the talcum powder and sieving through a screen with 80-140 meshes to obtain zinc oxide fine powder and fine talcum powder; filtering the edible sesame oil, heating a Vaseline in a water bath to 80-100 DEG C; mixing and stirring the zinc oxide fine powder and the fine talcum powder with the Vaseline heated in the water bath and the filtered sesame oil according to the weight ratio and uniformlyadjusting and milling; and adding the filtered sesame oil when the Vaseline heated in the water bath is mixed with the zinc oxide fine powder and the fine talcum powder or mixing the Vaseline with the filtered sesame oil first and heating the mixture in the water bath to obtain the high-point indication paste of the denture base. According to the invention, the uniformity of the mixed substance can be ensured, so that the texture of an indication agent is finer and smoother; the high-point indication paste is not easy to stick to a mucosa when the denture base is indicated at a high point, can ensure that the area required to be adjusted and changed is displayed more distinctly and a comfortable mouth feeling is obtained by a patient, has no stimulation on the local mucosa, is easily removed after being used, is not easy to deteriorate, and has long guarantee period; and the use cost can be reduced.
WO2013161820A1 Composition for promoting bifidobacteria growth The present invention provides a growth-promoting composition enabling favorable promotion of the growth of microbes belonging to the Bifidobacterium genus, which inhabit the intestines of mammals such as humans. According to the present invention, containing one or more species selected from the group consisting of lacto-N-tetraose, lacto-N-neotetraose, and derivatives thereof makes it possible to provide a composition for promoting growth of microbes belonging to the Bifidobacterium genus. The growth-promoting composition is suitable for promoting the growth of the enteral microbes by oral administration, especially in adult humans.
WO2010144646A3 Anti-viral compounds to treat hcv infection Compounds effective in inhibiting replication of Hepatitis C virus ("HCV") are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
WO2011143935A1 Crystalline of carbapenem derivative or its hydrate, preparation methods and uses thereof Disclosed are a crystalline of carbapenem derivative represented by formula (I) (4R,5S,6S)-3-[(3S,5S)-5-[(4-aminosulfonylphen-1-yl)methyl)aminoformyl]-3-pyrrolidinyl]thio-6-[(R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid or its hydrate, preparation methods thereof, their uses for manufacturing medicaments for preventing and/or treating infective diseases, and a pharmaceutical composition containing the crystalline.
WO2010063163A1 A patch of antiemetic agent A patch of antiemetic agent is disclosed. It comprises a backing layer, a strip layer and a drug-reservoir between the backing layer and the strip layer. The antiemetic composition in the drug-reservoir layer comprises an antiemetic agent, such as granisetron, ondansetron, palonosetron, tropisetron and dolasetron, an absorption enhancer and a pressure-sensitive adhesive.
US6921768 Cytostatic cerium compounds The invention relates to cerium compounds having general formulas (I) Rn i+Yi n− and (II) Rb +Yb + and their application as medicaments in the prophylaxis and/or treatment of cancer diseases. In formula (I), R is a group of general formula (A): and in formula (II), Rb is a group of general formula (B)
US7071170 Bactericides; antiprotozoa agents This invention relates to compounds of the formula wherein a, R1, R2, R3, R4, R5, R6 and X are each as defined above, and to pharmaceutically acceptable salts thereof, useful as potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating bacterial and protozoal infections by administering the compounds of formula I.
WO2011048070A1 Methods and pharmaceutical compositions for the treatment of disorders of glucose homeostasis The invention is in the field of disorders of glucose homeostasis therapy. In particular the invention relates to a CFTR inhibitor or an inhibitor of CFTR gene expression for use in the treatment of disorders of glucose homeostasis. The present invention also relates to an in vitro methods for increasing the pool of Ngn3+ endocrine progenitor cells, pancreatic endocrine cells, or β cell mass obtained from stem cells, wherein said methods comprises the step of contacting stem cells with a CFTR inhibitor or an inhibitor of CFTR gene expression. The present invention also relates to a method of testing a subject thought to have or be predisposed to having disorders of glucose homeostasis, which comprises the step of analyzing a sample of interest from said subject for: (i) detecting the presence of a mutation in the CFTR gene and/or its associated promoter, and/or (ii) analyzing the expression of the CFTR gene.
US20100063084 Multi-phase release methscopolamine compositions Formulations have been developed administering methscopolamine in multi-phases. In a preferred embodiment, the formulation contains methscopolamine in an immediate release. (“IR”) form and a sustained or delayed release (“DR”) form and/or poised release (“PR”) form. In another embodiment, the methscopolamine is released in a gradient, decreasing the side effects associated with rapidly elevated blood levels. In another embodiment the drug is bound to an ion-exchange resin, which can be suspended in a liquid or incorporated into a matrix for delayed, sustained and/or pulsed release. Dosage unit forms may be tablets, gels, liquids, capsules, beads, microparticles, films or lozenges. Multi-phase delivery can also be achieved through the use of a kit that provides for dosage escalation. This kit can be a blister pack or equivalent, wherein the drug is packaged so that a first dosage is taken, then sequentially larger dosages. The dosages can be the same in each unit, and instructions provided so that the correct dosage is obtained through the number of units and the time of administration or the dosages may be different, and the units ordered so dial the desired dosage administration profile is obtained when the patient takes the units in order as instructed.
CN1827604A Nitro compounds and their application in preparation of pemetrexed The invention relates to a nitro compound and process of its preparation, as well as the use in the preparation of pemetrexed, a kind of anti-tumor medicament, which has the advantages of simplified post-reaction treatment, high product purity, and facilitation of industrialized production.
WO2012052390A1 N-2-(2-pyridinyl)-4-pyrimidinyl-beta-alanine derivatives as inhibitors of histone demethylase jmjd3 A method of treating autoimmune diseases or conditions in a mammal, such as a human, which comprises the administration of a therapeutically effective amount of histone demethylase enzymes of formula (I).
US20120238609 Methods for Treating COPD Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for treating COPD.
CN101890165A Composition for lowering blood pressure and application thereof The invention provides a pharmaceutical composition which comprises calcium channel blockers of a medicinal dose, angiotensin II receptor antagonists of a medicinal dose, one or more of B vitamins of a medicinal dose and pharmaceutically acceptable carriers, wherein the calcium channel blockers are selected from amlodipine, felodipine, israbipine, nicardipine, nifedipine, nisoldipine, nitrendipine, lacidipine, diltiazem or verapamil; the angiotensin II receptor antagonists are selected from candesartan, telmisartan, losartan, valsartan, irbesartan, eprosartan, tasosartan or olmesartan; and the B vitamins are selected from one or more of vitamin B6, vitamin B12, folic acid and calcium leucovorin. The pharmaceutical composition of the invention can improve the curative effect of the hypotensor, enhance the target organ protecting action of the hypotensor, and reduce the morbidity of complications of angina, myocardial infarction and the like.
US7745622 Crystalline N-(4-(4-ammoniumthieno[2,3-d]pyrimidin-5-yl)phenyl)-N′-(2-fluoro-5-(trifluoromethyl)phenyl)urea benzenesulfonate A crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N′-(2-fluoro-5-(trifluoromethyl)phenyl)urea benzenesulfonate characterized in the triclinic crystal system and P-1 space group, when measured with radiation at 0.7107 Å, by lattice parameters a, b and c of 7.800 ű0.001 Å, 13.406 ű0.002 Å and 13.554 ű0.002 Å, respectively and α, β and γ of 67.155±0.002, 79.724°±0.002° and 84.067±0.002, respectively, ways to make it, compositions comprising it, and methods of treatment using it are disclosed.
US7101907 Topical administration of statins for treatment of bone disorders The topical administration of statins for the treatment of bone disorders is disclosed.
CN102020538A PTP1B (Protein Tyrosine Phosphatase 1B) inhibitor as well as synthesis method and application thereof to preparation of type 2 diabetes medicament The invention relates to a novel chemical total synthesis method of a PTP1B (Protein Tyrosine Phosphatase 1B) inhibitor and application thereof to a medicament for treating type 2 diabetes. The PTP1B inhibitor has the following chemical structural formula shown in the specification: radicals connected with carbon of 2,2', 3,3' and 6,6' bits of a benzene ring are bromine atoms, carbon of 4,4' and 5,5' bits are connected with hydroxyl, and the PTP1B inhibitor has the English name of bis-(2,3,6-tribromo-4,5-dihydroxy-phenyl)-methane. The compound has favorable treatment action on the type 2 diabetes of an insulin resistance type by restricting the activity of the PTP1B and enhancing the sensitivity of an insulin receptor.
CN101977605A Use of ranolazine for treating pain This invention relates to methods for treating a patient suffering from neuropathic or nociceptive pain which may be mechanical, visceral, and/or inflammatory in nature, comprising administering a therapeutically effective amount of Ranolazine to a patient in need thereof.
WO2007132852A1 Poorly-water-soluble pharmaceutical agent A particulate, poorly-water-soluble pharmaceutical agent having an average diameter of 50 to 200 nm; and a particulate complex comprising the particulate, poorly-water-soluble pharmaceutical agent and a polymeric electrolyte and having an average diameter of 50 to 250 nm.
US20110039819 Substituted phenoxybenzamides The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
WO2009074674A3 Trisubstituted piperidines as renin inhibitors The application relates to trisubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R1, R2', X, U, W, m and n have the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
CN102600130A New clinical use of oxiracetam and optical isomer of oxiracetam The invention provides a new clinical use of oxiracetam for treating epilepsy. Oxiracetam is an analogue of piracetam and a pyrrolidone derivative, and is clinically used for improving senile dementia and memory and learning functions of patients with dysmnesia. The results of mechanism studies imply that oxiracetam, especially laevo isomer of oxiracetam as L-oxiracetam, can promote synthesis of phosphorylcholine and phosphoethanolamine, increase ratio of ATP (adenosine triphosphate )/ADP (adenosine diphosphate) in brain, and increase synthesis of protein and nucleic acid in brain. The study finds that oxiracetam and optical isomer of oxiracetam can effectively inhibit unexpected abnormal discharge of cerebral neurons, thereby treating partial seizures of epilepsy.
US20110052710 Novel nanoparticles for delivery of active agents Milled nanoparticles comprising a biologically active agent, at least one biopolymer and a coating containing at least one coating which is a polymer or ligand are produced using milling and coating techniques which have not previously been used for these applications.
CN101390925A Composite immunity strengthening agent for fresh water young fish Disclosed is a compound immunopotentiator for freshwater fry, which is characterized in that the compound immunopotentiator is composed of by weight proportion: 25-35% of Beta-glucan, 20-30% of chitosan, 15-25% of bacillus subtilis, 10-15% of vitamin C, 8-13% of bupleurum, 7-11% of astragalus and 5-8% of eucommia ulmoides. The compound immunopotentiator has the advantages that: (1) the compound immunopotentiator is used as feed additive in fry feed with the addition of 0.1%-0.2%; (2) the immunity of fry is obviously enhanced and the survival rate is improved; (3) the immune effect is higher than the immune effect of single immunopotentiator; the immunosuppression phenomenon caused by the long-term application of single immunopotentiator is overcome so that the compound immunopotentiator can be used in the whole cycle of animal breeding; (4) the source of raw materials is stable; the raw materials have low price, and the production process is simple.
CN101084901A Staphylococcus inhibitor The invention belongs to biological technique field, and relates to chemical compound of formula I acting as staphylococal inhibitor and a method of the inhibitor as medicament for preventing or treating relevant bacterial infection disease. Biochemical and biological experiments have shown that the inventive chemical compound has strong binding force with target protein staphylococcus epidermidis or Staphylococcus aureus tryptophanyl-tRNA synthetase, can inhibit the activity of the synthetase, has small influence to human tryptophanyl-tRNA synthetase activity; and can inhibit the growth of staphylococcus epidermidis Staphylococcus aureus. It has no toxicity to mammalian cell at minimal inhibitory concentration. The inventive inhibitor can be used for preparing medicament for preventing or treating staphylococcal disease and preparating disinfectant liquid.
WO2012119506A1 Indolone derivatives, pharmaceutical compositions thereof, and preparation methods and applications thereof The present invention provides indolone compounds represented by formula I, and stereoisomers or pharmaceutically acceptable salts or hydrates thereof. The indolone compounds can block signal transduction by VEGF receptors, block the ability of vascular endothelial cells to form new blood vessels, inhibit tumor neoangiogenesis and prevent malignant tumor metastasis.
CN101695498A Medicament for protecting hepatic injury caused by paracetanol and application thereof The invention relates to a medicament for protecting hepatic injury caused by paracetanol, and the active component of the medicament is Panax Notoginseng Ginsenoside which is one of contents of radix pseudo-ginseng. The invention also relates application of Panax Notoginseng Ginsenoside in protecting the hepatic injury caused by paracetanol. Panax Notoginseng Ginsenoside can protect the hepatic injury caused by paracetanol of a hepatotoxic drug and has the action of preventing and protecting the hepatic injury. The invention widens the pharmacy function of radix pseudo-ginseng and has application potential in the field of preventing and protecting the hepatic injury.
US8048897 Cyclohexane derivative, prodrug thereof and salt thereof, and therapeutic agent containing the same for diabetes A cyclohexane derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity, metabolic stability, and safety; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, e.g., insulin dependent diabetes mellitus (type 1 diabetes) or noninsulin-dependent diabetes mellitus (type 2 diabetes), complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): (wherein A is —O—, —CH2—, or —NH—; n is an integer selected between 0 and 1; R6 and R7 each independently is hydrogen or C1-6 alkyl; m is an integer selected among 1-3; Q is selected among the following formulae Q1 to Q5; Ar1 is optionally substituted arylene or optionally substituted heteroarylene, provided that the heteroarylene may be bonded to an aromatic carbocycle or aromatic heterocycle to form a fused ring; and Ar2 is optionally substituted aryl or optionally substituted heteroaryl), a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, or the like each containing the compound.
US20090074754 Methods and compositions useful in the treatment of mucositis In certain aspects, the present invention provides compositions and methods for treating mucositis.
WO2006115244A1 4-bromoisoquinoline derivative and pharmaceutical preparation comprising the same Disclosed is a compound which has a potent inhibitory effect on Rho-kinase and is useful as a therapeutic agent for diseases including hypertension, pulmonary hypertension, cerebral vasospasm, angina pectoris, heart failure, arteriosclerosis, glaucoma, dysuria, asthma and erectile dysfunction. A 4-bromoisoquinoline derivative represented by the general formula (1), an acid-addition salt thereof or a solvate of the derivative or the salt.
US20120196890 4-substituted azaadamantane derivatives and methods of use thereof The invention relates to compounds that are 4-substituted azaadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
CN101327204A Use of emodic acid in preventing and treating fatty liver The invention provides a usage of a rhein acitive substance during the preparation of a compound for preventing, controlling or treating the fatty liver. The rhein acitive substance comprises rhein, salt or ester of rhein, which is physiologically or pharmacologically acceptable, rhein salt or ester hydrate or a rhein salt or ester mixture. Besides, the invention also provides a compound which comprises: 1) rhein, 2) the active substance of the rhein, which prevents and treats the fatty liver, and 3) a pharmacologically or bromatologically acceptable carrier. The experiment of the invention indicates that the rhein has a remarkable effect for treating the fatty liver.
US20120258954 ArylSulfonamide Based Matrix Metalloprotease Inhibitors The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
WO2010060215A1 2-(n-substituted piperazinyl) steroid derivatives Novel chemical agents of Formula I are described herein. More specifically, 2-(N-substituted piperazinyl) pregnane and 2-(N-substituted piperazinyl) androstane derivatives exhibiting cytotoxicity on a variety of cancer cell lines are disclosed herein. (I)
EP2280708A1 Mmp-2 and/or mmp-9 inhibitor The present invention provides a highly safe pharmaceutical preparation effective for diseases caused by MMP-2 and/or MMP-9. The pharmaceutical preparation contains, as an active ingredient, at least one member selected from the group consisting of thiazole derivatives represented by Formula (1): wherein R1 represents a phenyl group that may have 1 to 3 lower alkoxy groups as substituents on the phenyl ring, and R2 represents a pyridyl group that may have 1 to 3 carboxyl groups as substituents on the pyridine ring, and salts thereof. Such thiazole derivatives have MMP-2 and/or MMP-9 inhibitory activity.
WO2009015164A3 Piperidinyl derivatives as modulators of chemokine receptor activity The present application describes modulators of MIP-1α of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
CN101385796B New use of a formulation in improving cognition dysfunction and preventing and treating senile dementia The invention relates to a qingkailing preparation and the application of a composition of effective components thereof including baicalin, jasminoidin, cholic acid and mother of pearl to improving cognitive dysfunction, preventing and treating senile dementia. Morris water maze experiments prove that the qingkailing preparation and the effective components thereof can improve the cognitive dysfunction of senescence accelerated mice; an in-vivo experiments prove that the qingkailing preparation can improve plasticity change of Alzheimers disease model rats synapse damage resulting from A beta1-42 hippocampal injection; an in vitro experiments prove that the qingkailing preparation and the composition of the effective components thereof including baicalin, jasminoidin, cholic acid and themother of pearl can improve complete cerebral acetylcholine content of the senescence accelerated mice, can cause relative increment in the dopamine and serotonin levels of central nerve by staying the degradation of the acetylcholine, the dopamine and the serotonin, thus improving the intracerebral monoaminergic system activity, therefore, the Morris water maze experiments are possibly related to the effect of the qingkailing formula on improving the cognitive dysfunction and preventing and treating the senile dementia.
CN103222975A Application of enrofloxacin salt in preparation of swine oral preparation The invention discloses an application of enrofloxacin salt in the preparation of a swine oral preparation. The enrofloxacin salt is at least one of salts formed by enrofloxacin and metal ion. The metal ion is zinc, copper, calcium, magnesium, iron, cobalt, manganese, chromium, silver or nickel. The enrofloxacin salt formed by enrofloxacin and the metal ion can be used to remarkably improve palatability of pigs to enrofloxacin. It proves through pharmacokinetics and artificial disease treatment tests that the enrofloxacin salt formed by enrofloxacin and the metal ion will not influence bioavailability. Thus, an oral preparation medicated through an alimentary canal can be developed and used in pig production, not influencing normal ingestion of pigs.
US20110028497 Novel derivatives of purinic and pyrimidinic antiviral agents and use thereof as potent anticancer agents Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.
WO2009021728A3 Targeted block copolymer micelles The present invention provides a micelle comprising an amphiphilic block copolymer, said amphiphilic block copolymer consisting of (a) a hydrophobic polymer attached to the 5' end of a first nucleic acid molecule, wherein said first nucleic acid molecule is hybridized with a second nucleic acid molecule, wherein a targeting unit capable of selectively binding to a specific cell type and/or tissue is attached to the 5' end of said second nucleic acid molecule; and/or (b) a hydrophobic polymer attached to the 3' end of a first nucleic acid molecule, wherein said first nucleic acid molecule is hybridized with a second nucleic acid molecule, wherein a targeting unit capable of selectively binding to a specific cell type and/or tissue is attached to the 3' end of said second nucleic acid molecule.
WO2006040329A1 1 ibeta- hydroxysteroid dehydrogenase type 1 active spiro compounds A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11 β-hydroxy-Steroid dehydrogenase type 1 (11 βHSD1 ) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
WO2008086783A3 Platinum complex The invention relates to a reaction product of a platinum complex or a derivative thereof that is effective as a chemotherapeutic agent and a saccharide compound or a derivative thereof. The invention also relates to uses of the reaction product.
US8461331 Method for the production of 3,6-dihydro-L, 3, 5-triazine derivatives from metformin and paraldehyde derivatives Process for the preparation of compounds of the formula I in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in claim 1, which comprises the reaction of a compound of the formula II in which R1, R2, R3, R4 have the meanings indicated above, with a compound of the formula III in which R5, R6 have the meanings indicated above.
WO2009017454A1 New therapeutic combination of a gsk3 inhibitor and an a7-nicotinic agonist 960 The present invention related to a combination of (a) a GSK3 inhibitor and (b) an α7- nicotinic agonist. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treating CNS disorders in mammals by administrating said combination. The invention further relates to a kit comprising the combination and use of said kits in treatment of CNS disorders such as dementia and/or Alzheimer's Disease.
CN102716112A Pharmaceutical composition capable of resisting HPV (human papillomavirus) infection The invention belongs to the technical field of medicines and provides a pharmaceutical composition capable of resisting HPV (human papillomavirus) infection. The pharmaceutical composition capable of resisting HPV infection comprises germacrone, furanodiene, curdione, beta-elemene, curcumol, curzerene and borneol. The components of the pharmaceutical composition are definite, and the quality can be controlled. The weight part of the curzerene is controlled, thus the irritation of the medicine is reduced. The pharmaceutical composition can be used for preparing suppositories, ointments, capsules, effervescent tablets, gels, lotions and film or foam agents. The pharmaceutical composition has a good effect of treating HR-HPV (high risk human papillomavirus) and/or LR-HPV (low risk human papillomavirus) infection and other diseases and can be used widely clinically.
WO2010022358A8 6-substituted 2-(benzimidazolyl)purine and purinone derivatives and 6-substituted 2-(imidazolo[4,5- c]pyridinyl)purine and purinone derivatives for immunosuppression The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the genera formulae I and II wherein R1, R2, R3, R4, R9, Q, A and y are as defined in the specification.
WO2012062996A1 Derivatives of 6-amino-6-deoxyglucosamine and use of same as antibacterial agents The invention relates to compounds of formula (I) where: R1 ≠ 2-deoxystreptamine and the derivatives thereof substituted in positions 5 and/or 6; R2 and R6 are the same or different and represent a primary, secondary or tertiary amine function: NH2, NHR, NRR' where R and R' = alkyl, aryl, cyclic or otherwise, substituted or otherwise; OR3 and OR4 form alcohol, ether, ester, carbonate, carbamate, sulfonate or sulfamate functions; and if R3 = R4, then R3 and R4 ≠ H; if R3 = H, then R4 ≠ H and R1 ≠ OH; and if R4 = H, then R3 ≠ H and R1 ≠ OH; if R1 = OH, then R3 and R4 ≠ H, and if R1 = OR5, then R3 and/or R4 and/or R5 are not a sugar or a polysaccharide. The invention further relates to the use of said compounds as drugs and, specifically, as antibiotics.
US7435595 Using prokaryotic histone protein as tool in transfer of heterologus nucleotide sequences into cells; improving exogenous gene expression The invention relates to a method for the transfer of molecular substances, for example proteins or nucleic acids in cells, in the case of using DNA combined with a possible gene expression. A prokaryotic nucleic acid-binding protein is used for the transfer, which is preferably obtained from a thermostable organism. Where the substance to be transferred is a nucleic acid, the protein forms a reversible complex with the nucleic acid. The prokaryotic protein condenses and compacts the nucleic acids. Said nucleic acids can be taken up in the target cells after suitable incubation.
CN1837197A Salvianolic acid M and rosmarinic acid as aldose reductase inhibitor in sage The invention discloses an aldose reductase inhibitor pellet phenolic acid M and rosmarinic acid of sage, which is characterized by the following: IC50 of pellet phenolic acid M is 0.79 mug/mL; IC50 of rosmarinic acid is 1.13 mug/mL; the pellet phenolic acid M or extract with pellet phenolic acid M, rosmarinic acid or extract with of rosmarinic acid can prevent an cure diabetes complication.
EP0871487B1 Dendritic cell stimulatory factor Flt3-ligand can be used to generate large numbers of dendritic cells from hematopoietic progenitor and stem cells. Flt3-ligand can be used to augment immune responses in vivo, and expand dendritic cells ex vivo. Such dendritic cells can then be used to present tumor, viral or other antigens to naive T cells, can be useful as vaccine adjuvants.
CN102038913A Oral preparation for treating cerebral apoplexy and preparation method and application thereof The invention discloses a medicinal composition for treating medium convalescent nerve function defect of cerebral apoplexy, a preparation method for the medicinal composition and medicinal application of the medicinal composition in preparation of a medicament for medium and posterior nerve function defect of cerebral apoplexy. Natural musk is replaced by adopting artificial musk so as to reduce the application cost and save resources; and the volatile oil is extracted by adopting supercritical fluid technology, effective ingredients are refined and purified by adopting macroporous absorption resin technology, and the effective ingredients are high and have good treatment effect on the medium convalescent cerebral apoplexy, particularly medium and posterior nerve function defect of cerebral apoplexy.
CN103735570A Oral care solution for preventing oral fungal infection The invention discloses an oral care solution. The oral care solution comprises 1-5% of sodium bicarbonate, 0.006-0.02% of vitamin B1, 0.003-0.02% of vitamin B2, 0.0004-0.002% of vitamin B6, 0.02-0.1% of nicotinamide, 0.002-0.01% of calcium pantothenate, 5,000,000,000-20,000,000,000/100kg of nystatin dehydrate and the balance of water. The oral care solution has a broad-spectrum antifungal effect, is high in antimicrobial activity on mycotoruloides, small in local drug concentration, and small in toxic and side effects on a suffer with incomplete liver and kidney functions, not only can be applied to prevention of the oral local infection, but also can be applied to treatment of fungal infection.
US20050059698 Cognitive and attention deficit symptoms of Alzheimer's, neurodegeneration disease, behavioral or psychological disorders; N-((3R)-1-azabicyclo[2.2.2]oct-3-yl)-2,3-dihydro-1,4-benzodioxine-6-carboxamide L-malate; including antipsychotic drugs The invention provides the malate salt of compounds of Formula I: A-NH-C(O)-B.X Formula I wherein X is malate salt, including D- or L-; wherein A is wherein B is or pharmaceutical composition, racemic mixture, or pure enantiomer thereof. The compounds of Formula I are useful to treat diseases or conditions in which α7 is known to be involved.
US20090247463 Polymer-based sustained release device This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.
US20130129808 Medical product containing active component of propolis or grapefruit seed extract and manufacturing method thereof A medical product containing either an active ingredient of propolis which is a natural antibiotic or a grapefruit seed extract, and a manufacturing method thereof are provided. The medical product is impregnated with a solution of CAPE (caffeic acid phenethyl ester) or pinocembrin, which is an active ingredient of propolis having antibacterial effects, to increase the antibacterial activity of the medical product due to antibacterial compounds contained in the active component, or the medical product is impregnated with a solution of a grapefruit seed extract such that the extract can exhibit antibacterial activity in the medical product.
CN103648530A Protein-active agent conjugates and method for preparing the same The invention provides protein- active agent conjugates having an amino acid motif that can be recognized by an isoprenoid transferase. The invention also provides compositions containing the conjugates, as well as methods for making the conjugates and compositions. The invention further provides methods for using the conjugates to deliver the active agent to a target cell, as well as methods for using the conjugates to treat a subject in need thereof (e.g., a subject in need of the active agent).
CN101596179A Medicament composition for treating hyperammonemia and preparation method thereof The invention provides a medicament composition for treating hyperammonemia and a preparation method thereof. The medicament composition uses an extractive glutamic acid as an active component and is an extractive glutamic acid injection used for treating the hyperammonemia caused by acute and chronic liver diseases, such as cirrhosis, fatty liver and hepatitis, and is specially suitable for eliminating central nervous system symptoms caused by the liver diseases and the emergency treatment of hepatic coma.
WO2008098396A3 Oxazolidinones and their use as hypocholesterolemic agents The present invention relates to novel hypocholesterolemic compounds of formula (I) useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels as well as to pharmaceutical compositions comprising said compounds alone or in combination with other active agents.
US7947697 8-(3-pentylamino)-2-methyl-3-(2-chloro-4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[d] pyrazolo[1,5-a]pyrimidine methanesulfonate as a CRF antagonist 8-(3-pentylamino)-2-methyl-3-(2-chloro-4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidine methanesulfonate of the structural formula (I) has Corticotropin Releasing Factor (CRF) antagonist activity and is useful in treating neuropsychiatric and digestive system diseases.
WO2006108949A3 Novel use of zinc gluconate for treating hydradenitis suppurativa The invention concerns a novel therapeutic use of zinc gluconate. Zinc gluconate is used in an orally deliverable form, in accordance with a daily dose schedule between 45 and 125 mg, for treating hydradenitis suppurativa, or Verneuil's disease.
EP2477631A1 Substituted phenylamine carboxamide analogs as mglur5 negative allosteric modulators and methods of making and using the same Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
WO2010126169A1 Pharmaceutical composition for preventing vascular disorders which comprises alk1 inhibitor as active ingredient Disclosed is use/usage of an activin receptor-like kinase 1 (ALK1) inhibitor in a pharmaceutical composition for preventing vascular disorders. Specifically disclosed are: a pharmaceutical composition for preventing vascular disorders, which contains an ALK1 inhibitor as an active ingredient; and a method for treating vascular disorders using the pharmaceutical composition.
CN103393628A Application of muscarinic receptor 3 in treating prostatic cancer The invention provides an application of a muscarinic receptor 3 as a drug target in treating prostatic cancer. The application has the advantages that high expression of CHRM3 (Muscarinic Acetylcholine Receptor 3) in tumor of prostate is discovered for the first time, and CHRM3 is activated to promote proliferation and migration of tumor of prostate and is inhibited as the drug target to inhibit growth and migration of tumor of prostate. CHRM3 is inhibited as an important clinical therapeutic target for treating prostatic cancer, so that huge social and economic benefits are brought.
US6867176 Method for preparing zinc-oligopeptide easily absorbable by the human body Disclosed is a method for preparing zinc-oligopeptides easily absorbable by the human body. A suspension of protein in deionized water at a neutral pH range in the presence of a protease is subjected to proteolysis to give a mixture of oligopeptides. Zinc ions are chelated with the oligopeptides to give a zinc-oligopeptide solution. The zinc-oligopeptide solution is concentrated and dried to a powder. Also provided is a beverage or food composition containing the zinc-oligopeptide, which can make contribution to avoid the lack of dietary zinc.
US20110257107 Compounds for Delivering Amino Acids or Peptides with Antioxidant Activity into Mitochondria Disclosed are compounds containing single amino acids, peptides, or derivatives thereof which are selectively delivered to the mitochondria of a cell. Compounds of the invention exhibit antioxidant activity thereby reducing reactive oxygen species in cells. These compounds are useful for inhibiting oxidative stress-induced cell injury or death both in vivo and ex vivo. In addition, methods for the synthesis of these compounds are disclosed.
WO2007066068A3 Calcium ion channel receptor antagonist The invention relates to pharmaceutically useful agents that antagonize the activity of a calcium ion channel receptor and their use in the inhibition of receptor activation in the treatment of conditions that would benefit from said inhibition; and including screening assays to identify antagonists of receptor activation and other subject matter. The agent may be a pheniramine.
CN101385735B Pharmaceutical use of morroniside The invention relates to a preparation method of morroniside and a new use thereof, in particular to the application of the morroniside in the preparation of drugs for preventing or treating acute and chronic liver injury and liver fibrosis and the preparation method of the morroniside.
EP2147914A1 Aminodihydrothiazine derivatives substituted with cyclic groups This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid β protein.
EP2334178A1 Compositions and methods for the treatment of bowel diseases with granulated mesalamine Disclosed are methods for treating gastrointestinal disorders, e.g., Crohn's disease, ulcerative colitis, and diverticular disease, with a granulated mesalamine formulation. Some formulations use granulated mesalamine in capsule form. Also included are methods to extend remission of ulcerative colitis by administration of a once -daily dosage of granulated mesalamine.
US7078408 administering pyrimidinotriazole derivatives for improving motor impairment due to Parkinson's Disease Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1–C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted-aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations
WO2008069922A1 Compositions including triciribine and anthracyclin analogs and methods of use thereof This application relates to combination therapies including triciribine and related compounds and anthracycline analogs and salts thereof and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
US20100292289 Treatment of metabolic syndrome with novel amides The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention.
EP2301945A1 Hydrates of erythromycin salts, the preparation and the use thereof The present invention relates to a macrolide derivative as well as preparation and use thereof. The macrolide derivative of the present invention, i.e., a hydrate of erythromycin salts, has a molecular formula of C37H67NO13·A·nH2O, n=1.0-11.0, in which A is an organic acid or an organic acids, selected from lactobionic acid, thiocyanic acid, maleic acid, fumaric acid, thiocyanic acid, acetic acid, methanesulfonic acid, benzenesulfonic acid, nicotinic acid, lactic acid, citric acid, tartaric acid, aspartic acid, glutamic acid and phosphoric acid, the hydrate has good water solubility and better storage stability, which is suitable for the manufacture of a medicament for the treatment and prophylaxis of infectious diseases in human or animal caused by Gram-positive or negative bacteria.
WO2007033265A1 Dipeptidyl peptidase inhibitors for treating diabetis Pharmaceutical compositions comprising 2-[[2-[(3R)-3-Amino-piperidinyl)-5-fluoro-6-oxo-6H-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.
CN101870720A Preparation method of ursolic acid and application thereof to medicine treating tumor diseases The invention discloses a preparation method of ursolic acid and application thereof to medicine treating tumor diseases. The ursolic acid has a molecular formula of C30H48O3, and the molecular weight of 456. The preparation method comprises the following steps: drying raw materials of oldenlandia diffusa; pulverizing whole plants of the oldenlandia diffusa; then, respectively using ethyl acetate and ethanol for extraction; merging obtained extracts; making the materials pass through a positive phase post and an RP-C18 reverse phase post for carrying out separation; then, adopting an n-hexane-ethyl acetate-methanol-water reverse flow chromatographic resolution system for collection; and obtaining ursolic acid monomers after the solvents are volatilized. The ursolic acid prepared by the invention has obvious anti-tumor activity on human liver cancer multi-drug-resistance cells when being used as signal preparations or medical dressing combinations, and the acting mechanism is a caspase independent cell apoptosis path mediated through AIF. The ursolic acid has low toxicity, so the ursolic acid has good application prospects of clinical tumor chemotherapy, particularly the anti-clinical tumor multi-drug resistance.
CA2115828C Calcium receptor active molecules Method and composition useful for treating a patient having a disease characterized by an abnormal level of one or more components, the activity of which is regulated or affected by activity of one or more Ca2+ receptors. Novel compounds useful in these methods and compositions are also provided. The method includes administering to the patient a therapeutically effective amount of a molecule active at one or more Ca2+ receptors as an agonist or antagonist. Preferably, the molecule is able to act as either a selective agonist or antagonist at a Ca2+ receptor of one or more but not all cells chosen from the group consisting of parathyroid cells, bone osteoclasts, juxtaglomerular kidney cells, proximal tubule kidney cells, keratinocytes, parafollicular thyroid cells and placental throphoblasts and a pharmaceutically acceptable carrier.
US20090004145 Compositions and methods involving gene therapy and proteasome modulation The present invention concerns the methods and compositions involving a therapeutic polypeptide, such as a tumor suppressor or a nucleic acid encoding such in combination with a proteasome inhibitor, for the treatment of cancer. In certain examples, a treatment for ovarian cancer is provided.
US7317020 Isolation and structure of Cribrostatin 6 Cribrostatin 6, a dark blue cancer cell growth inhibiting constituent of the Republic of Maldives marine sponge Cribrochalina sp. has been isolated, and its structure (shown below) elucidated, based on a combination of RMS, high field (500 MHz, HMBC, and GOESY experiments) 15N, 1H- and 13C NMR, and X-ray crystal structure analyses. Cribrostatin 6 also was found to inhibit the growth of a number of pathogenic bacteria and fungi.
EP2666358A1 Treating Psychological Conditions Using Muscarinic Receptor M1 Antagonists Provided are methods of treating psychological diseases and conditions by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.
US6995147 Method of delaying the onset of diabetes A method for preventing, delaying the onset of or treating diabetes in a patient comprising selecting a patient who is susceptible to developing diabetes, who is developing diabetes or who is diabetic and administering to the patient one or more than one dose of a pharmaceutical agent comprising a polynucleotide encoding a secreted exogenous protein, such as a secreted luciferase or a secreted form of human glutamic acid decarboxylase.
DE102006058243A1 Pharmaceutical composition, useful prophylaxing and/or treating e.g. metabolic syndrome, diabetes mellitus, liver diseases, chronic-inflammatory diseases, rheumatic diseases, comprises a combination of pomegranate preparation and selenium Pharmaceutical composition comprises a combination of a pomegranate preparation and selenium. - ACTIVITY : Metabolic; Antidiabetic; Hepatotropic; Antiinflammatory; Antirheumatic; Hypotensive; Cardiant; Vasotropic; Cardiovascular-Gen; Antiarteriosclerotic; Virucide; Osteopathic; Neuroprotective; Nootropic; Cytostatic; Anabolic. - MECHANISM OF ACTION : None given.
US20050032815 Preventing dermatitis in a human by administering a composition consisting of therapeutically effective amounts of optically pure (-) cetirizine or salt thereof, and a leukotriene inhibitor or salt thereof; synergistic mixture; also useful as asthma treatment Methods and pharmaceutical compositions employing (+) cetirizine, (−) cetirizine, or racemic cetirizine, or a pharmaceutically acceptable salt thereof, and a leukotriene inhibitor, or a pharmaceutically acceptable salt thereof, or decongestant for the treatment, management, and/or prevention of inflammation, asthma or symptoms thereof, allergic disorders such as allergic rhinitis, and dermatitis.
US7456195 Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
WO2010090234A1 12-deoxyfusicoccin sugar chain-modified derivatives and uses thereof Disclosed are novel water-soluble compounds that have differentiation-inducing effects on mammalian cells, cell differentiation-inducing agents that have said compounds as active ingredients and anti-tumor agents. Disclosed are compounds and salts thereof that are represented by general formula (1) (1) (wherein n represents an integer 0‑5, Me a methyl group, and R1 a 1- to 6-carbon alkyl group or amino group represented by formula (2) (2) (wherein R2 represents a hydrogen atom or 1- to 6-carbon alkyl group, R3 a hydrogen atom, 1- to 6-carbon alkyl group, a 1- to 7-carbon acyl group or amidyl group (–CNHNH2)])
US7053077 such as estrone sulfamate and/or estradiol sulfamate for oral administration or for use in intrauterine releasing system (IUD) The invention relates to the use of biogenic estrogen sulfamates for the oral discontinuous application for hormone replacement therapy (HRT). The discontinuous administration takes place in intervals ranging from 2 to 40 days. The invention also provides the additional application of gestagens, preferably continuously in the form of an implant or in the form of an intrauterine releasing system (IUD). Estrone sulfamate, estradiol sulfamate or an N-acyl sulfamate of estrone, estradiol or estriol having up to 7 C-atoms in the acyl chain, or a combination comprised of two or more of said active ingredients are used as biogenic estrogen sulfamates.
US20070259961 Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal or cancer Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory diseases, immunological diseases and cancer.
CN102688316A Livestock compound medicine with anti-virus and immune regulation functions The invention discloses a livestock compound medicine with anti-virus and immune regulation functions. The livestock compound medicine is prepared from astragalus root, codonopsis pilosula, angelica, hedyotis diffusa, honeysuckle, radix bupleuri, liquorice and Isoprinosine. The livestock compound medicine has the functions of invigorating spleen-stomach and replenishing qi, replenishing blood, invigorating the circulation of blood, strengthening spleen and tonifying lung, clearing away heat and toxic materials, protecting liver, anti-inflammatory and reinforcing the organism immunity and has excellent treatment effect on various immune suppression diseases of livestock. The livestock compound medicine can improve the organism immunity of livestock, reinforce the cell immunity of livestock, promote the antibody generation, eliminate the organism immunity inhibition and effectively prevent and treat the livestock virosis. After use, the livestock compound medicine can promote the lymphocyte proliferation, increase the phagocytotic ability of phagocyte, reinforce the organism immunity of livestock, eliminate the organism immunity inhibition and greatly reduce the injury of immunosuppressive diseases to the livestock organism. The livestock compound medicine has no medicine residue, meets the safety and health requirements of livestock foods and is convenient to use; the livestock compound medicine can be taken together with drinking water or can be mixed with feed without affecting the export of such animal products as livestock products.
CN1879641A Dispersible tablet of glycyrrhizin and preparation method thereof The invention relates to a glycyrrhizin dispersible tablet and method for preparation, wherein the formula comprises (by weight ratio) glycyrrhizin 25-300, filling agent 15-350, crumbling agent 15-250, lubricating agent 1-10, and right amount of wetting agent or binding agent. The crumbling agent is one selected from the following or their various combination: sodium carboxymethylstarch, crosslinked povidone, cross-linked sodium carboxymethylcellulose, or low substituted methylcellulose propylene glycol ether. The filling agent is one selected from the following or their various combination: lactose, crystalline cellulose, starch, starch gum, mannitol. The lubricating agent is one selected from the following or their various combination: magnesium stearate, talcum powder, magnesium dodecylsulfate, sodium dodecylsulfate, miropowdered silica gel. The tablet also comprises right amount of wetting agent or binding agent, the wetting agent or binding agent being one of water, 10-95% ethanol, and 10% polyvinylpyrrolidone-K30.
CN102887894A Crystal form of solifenacin succinate and preparation method thereof The invention provides a novel crystal form of (3R)-1-azabicyclo[2.2.2]octan-3-yl(1S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate butanedioic acid (solifenacin succinate, YM905) which is characterized in that an X-ray powder diffraction spectrum represented in degree of 2[theta] has characteristic peaks at positions of 3.5 +/- 0.2, 7.1 +/- 0.2, 10.8 +/- 0.2, 18.3 +/- 0.2, 21.5 +/- 0.2, 22.1 +/- 0.2, 24.9 +/- 0.2 and 35.5 +/- 0.2. The invention further provides two preparation methods of the solifenacin succinate with such crystal form. A first method is characterized by comprising the following steps: heating and dissolving the solifenacin succinate in acetone, adding a certain amount of ethyl acetate, cooling and crystallizing to obtain the solifenacin succinate with such crystal form; and a second method is characterized by comprising the following steps: dissolving a certain amount of solifenacin in isopropanol under a certain temperature, adding a certain amount of succinic acid, stirring to react, cooling and crystallizing to obtain the solifenacin succinate with such crystal form.
CN101756970A Sustained release preparation containing memantine hydrochloride and huperzine A and preparation method thereof The invention relates to sustained release preparation containing memantine hydrochloride and huperzine A and preparation method thereof. The sustained release preparation includes quick release component and slow release component, wherein the memantine hydrochloride is the quick release component which represents the characteristic of quick release in vitro dissolution test and can be released by more 80% 30min later, while huperzine A represents the characteristic of slow release in vitro dissolution test and is released by 10-30% in the first hour, by 40-60% in 6 hours, by 60-80% in 12 hours and by more than 80% in 18 hours. The sustained release preparation is mild, has long-term effect and can reduce the application time (only once a day) and improve the compliance of the patient. The invention further discloses the vitro release characteristic and the preparation method of the sustained release preparation.
US20090048233 Enhancing the Tolerability of a Seratonin Antagonist and a NSRI, a SNRI or a RIMA by Using Them in Combination Provided are combinations of pharmaceutical agents capable of eliciting a therapeutic effect. A first therapeutic agent in the combination has 5HT2/5HT3 antagonist and alpha-2 antagonist activity. A second therapeutic agent possesses both serotonin reuptake inhibitory activity and norepinephrine reuptake inhibitory activity or is a reversible inhibitor of monoamine oxidase A (RIMA). In some embodiments, a combination of a first therapeutic agent and a second therapeutic agent results in reduction in one or deleterious side effects associated with the first therapeutic agent, the second therapeutic agent or both. Also provided are methods of treatment employing a first therapeutic agent and a second therapeutic agent. Also provided are kits containing a first therapeutic agent, a second therapeutic agent and instructions for administering the first therapeutic agent and the second therapeutic agent.
WO2007127502A3 Polymorphic form of { 2-methyl-4- [ 4-methyl-2- ( 4-triflu0r0methylphenyl) thiazol -5- ylmethylthiol phenoxy }-acetic acid The present invention relates to a novel polymorphic form of the compound {2- methyl-4-[4-methyl-2-(4-trifluoromethyl phenyl) thiazot-5-ylmethylthio]phenoxy}-acetic acid, methods of preparing it, pharmaceutical compositions and medicaments containing the same, and use of such polymorphs, compositions and medicaments in the treatment of PPAR mediated diseases or conditions.
US20120039986 Compositions and methods for sirna inhibition of angiopoietin 1 and 2 and their receptor tie2 RNA interference using small interfering RNAs which are specific for mRNA produced from the Ang1, Ang2 or Tie2 genes inhibits expression of these genes. Diseases which involve Ang1, Ang2 or Tie2 mediated angiogenesis, such as inflammatory and autoimmune diseases, diabetic retinopathy, age related macular degeneration and many types of cancer, can be treated by administering the small interfering RNAs.
US20100267704 Autophagy Inducing Compounds and Uses Thereof in Treating Autophagy Associated Diseases This invention pertains to a class of autophagy inducing compounds that treat diseases caused by misfolded protein aggregates and a screening method for identifying these compounds.
CN102241671A Precursor phase and use thereof for preparing the magnesium tetrahydrate salt of an omeprazole enantiomer The invention relates to a precursor phase and use thereof for preparing the magnesium tetrahydrate salt of an omeprazole enantiomer. A precursor phase of the magnesium tetrahydrate salt of an omeprazole enantiomer, and also processes for preparing it and its use for the preparation of the magnesium tetrahydrate salt are described. Crystals of the magnesium tetrahydrate salt thus obtained, and their uses, especially in the synthesis of the dihydrate form A of the magnesium salt of the enantiomer or as medicament are also disclosed.
EP1752147A1 Drug for prevention or treatment of diabetes The present invention provides a medicine for preventing or treating a diabetes, which includes 2,2-dichloro-12-(4-chlorophenyl)-dodecanoic acid or a pharmacologically acceptable salt thereof, and metformin as active ingredients. The present invention provides a method for preventing or treating a diabetes, which includes administering 2,2-dichloro-12-(4-chlorophenyl)-dodecanoic acid or a pharmacologically acceptable salt thereof, and metformin to a patient suffering from or having a possibility of suffering from diabetes.
CN103420877A Selective hydroxamate-based MMP inhibitors The present invention relates to selective hydroxamate-based MMP inhibitors. Specifically, the present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
CN102716413A Medicament for treating functional dysmenorrhoea A medicament for treating functional dysmenorrhoea belongs to the technical field of medical preparations. The invention employs the following technical scheme that each medicament comprises medicaments consisting of the following effective components: 200 to 300 grams of a curcuma, 5 to 15 grams of a cowherb seed, 20 to 70 grams of a lychee seed, 1 to 2 grams of borneol and 5 to 10 grams of liquor, wherein an optimum component ratio is 250 grams of the curcuma, 10 grams of the cowherb seed, 50 grams of the lychee seed, 1 gram of the borneol and 5 grams of the liquor. The medicament has efficacy of clearing heat, invigorating blood, dispelling cold, activating collaterals, relieving pain, promoting qi circulation and relieving depression and resolving carbuncle and dissipating stasis, and has effects of promoting blood circulation.
US20080242681 N-4-(6-(Hetero)Aryl-Pyrimidin-4-Ylaminophenyl)-Benzenesulfonamides as Kinase Inhibitors Compounds of a certain formula 1 in which R1 and R2 have the meanings indicated in the description are novel kinase inhibitors. Formula (1), in which R1 is phenyl, phenyl substituted by R3 and/or R4, naphthalenyl, naphthalenyl substituted by and/or R6, aryl1, aryl1 substituted by R7 and/or R8, R9, R10 or R11, R2 is phenyl, phenyl substituted by R12 and/or R13, naphthalenyl, naphthalenyl substituted by R14 and/or R15, aryl2, aryl2 substituted by R16 and/or R17 or a radical selected from Formula (2).
WO2009080200A1 Novel sulphoximide-substituted quinoline and quinazoline derivatives as kinase inhibitors Novel sulphoximide-substituted quinoline and quinazoline derivatives as kinase inhibitors The present invention relates to quinoline and quinazoline derivatives of the general formula (I) in which W, Y, R3 and R4 are indicated in the description and the claims, the use of the compounds of the general formula (I) for the treatment of various disorders, the preparation of compounds of the general formula (I), and intermediates useful in the preparation of compounds of the general formula (I).
US20120178749 Ns1 protein inhibitors The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention.
US7384955 N-[1-(cyclohexylmethyl)-2-[(4-ethoxyphenyl)methyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]-2,2-dimethyl-propanamide; cannabinoid CB1/CB2 receptor agonists; analgesic; in therapy, in particular in the management of pain Compounds of formula I or pharmaceutically acceptable salts thereof Formula (I) wherein Ar, R1, R2, R3, Ra, Rb and X are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain
US20120220554 Combretastatins for Prevention of Posterior Capsule Opacification Methods and compositions for the treatment and prevention of posterior capsular opacification are provided. The method comprises administering a therapeutically effective amount of a combretastatin to a subject suffering from or at risk of developing posterior capsule opacification.
EP2025347A1 Prophylactic and therapeutic agent for cancer A Ras, Raf, MEK, ERK or RSK inhibitor, namely a P-glycoprotein expression inhibitor or a BCRP expression inhibitor, can be screened by utilizing the MAPK signaling activity as an indicator. It becomes possible to provide an anticancer agent which is reduced in resistance acquisition, and also provide an agent for preventing the resistance against an anticancer agent, which can enhance the therapeutic effect of the anticancer agent against cancer.
WO2013126993A1 Screening assays for identifying and validating agents that target cancer stem cells Described are methods for the identification and validation of an agent that specifically targets cancer stem cells (CSCs), but has no effect on normal stem cells (NSCs). The agent is identified by its ability to inhibit cell proliferation, or induce cell differentiation or death, of a surrogate CSC (sCSC) while having no such effect on the NSC. The sCSC is a human embryonic stem cell that has spontaneously acquired transformed characteristics but retains pluripotency (t-hPSC), or is a transformed induced-pluripotent stem cell (t-iPSC). Dopamine receptors (DRs) are identified as biomarkers for cancer stem cells. Antagonists of DRs induce differentiation of CSCs, eradicating their potential to seed cancer.
US20110178171 Compounds for cancer therapy A method of inhibiting the cellular proliferation of at least one selected from the group consisting of androgen dependent prostate cancer cells, androgen independent prostate cancer cells, oral cancer cells, liver cancer cells (hepatoma), and gastric cancer cells in a subject is provided, wherein the method comprises administrating to the subject an effective amount of an active component selected from the group consisting of Z form isochaihulactone (Z-K8) of the following formula (I), E form isochaihulactone (E-K8) of the following formula (II), a pharmaceutically acceptable salt of Z-K8 or E-K8, a pharmaceutically acceptable ester of Z-K8 or E-K8, and combinations thereof: and R is H, alkoxy, or aryl. Also provided is a method for manufacturing Z-K8 and E-K8.
EP2473482A1 Methods of treating orthomyxoviral infections Provided are novel iminosugars and methods of treating and/or preventing a disease or condition caused by or associated with a virus belonging to the Orthomyxoviridae family using iminosugars, such as DNJ derivatives.
US20120095015 Triazole compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor The invention relates to compounds of formula (I), wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of there compounds. The invention also relates to a pharmaceutically composition that comprises at least one triazole compound of the formula (I) and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula (I) to a subject in need thereof.
WO2005103011A1 Processes for preparing substituted n-aryl-n’-[3-(1h-pyrazol-5-yl) phenyl] ureas and intermediates thereof The present invention is directed to processes for the preparation of substituted phenylpyrazole ureas of Formula (I), that are useful as 5-HT2A serotonin receptor modulators for the treatment of disease.
US7655653 Tetrahydrobenzfluorene derivatives A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ′Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor β selective medical treatments.
EP2437758A1 Bacteria thya(-) mutants with increased vitamin k Bacteria thyA(-) mutants with increased vitamin K and use of these thyA(-) mutants for making a composition/product for treatment and/or prevention of vitamin K deficiency in a mammal (e.g. a human).
CN102885770A Novel gatifloxacin eye drop and preparation method thereof The invention discloses a novel gatifloxacin eye drop and a preparation method thereof. The preparation method of the eye drop disclosed by the invention comprises the steps of: dissolving gatifloxacin and relevant accessories in water; adding a swelling carbomer aqueous solution to the liquid medicine and then uniformly stirring; adding a sufficient amount of water; and finally, filtering and dispensing to obtain the eye drop. According to the novel gatifloxacin eye drop and the preparation method thereof, the defects of the current gatifloxacin eye drop are overcome; the residence time of the medicine on ocular surface is prolonged by the physical thickening and moisturizing lubrication effects of carbomer; and furthermore, the medicine seldom flows into mouth and nasal cavity so as to reduce medicine loss and avoid bitterness from the gatifloxacin eye drop, and therefore, compliance of patients is increased and clinical curative effect is ensured.
US20110059969 Piperazines as anti-obesity agents The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds, to processes for their preparation, and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
CN1634090A Nerve cell apoptosis resisting function of ganglioside GD1b and its application Disclosed is the neurocyte apoptosis resistant action of human endogenous compound, more specifically, the invention relates to the neurocyte apoptosis resistant action of ganglioside GD1b for adjusting potassium ion channel activity. In addition, the invention also relates to the use of the ganglioside GD1b in preparing neurocyte apoptosis resistant medicament for the prevention and treatment of nerve retrogression diseases, and the important use in preparing medicament for the prevention and treatment of potassium ion channel diseases.
CN101590223B SOD complex capsule and preparation method thereof The invention relates to an SOD complex capsule and a preparation method thereof. The SOD complex capsule contains resveratrol, coenzyme Q10, goose liver extracts, wheat germ extracts, safflower extracts and tartary buckwheat extracts; the weight ratio of the components is 10-50 : 10-75 : 75-150 : 75-150 : 75-150 : 200-500; every 100g of the complex capsule contains 40000-4000000 activity unit ofSOD which is a tadpole extract. The preparation method is as follows: processing grape skins, pig hearts, goose livers, wheat, safflower, tartary buckwheat and tadpole by the steps of breaking, concentration, centrifugal separation, purification and the like to obtain active ingredients of various raw materials, embedding the tadpole extract for several times, mixing the tadpole extract with other components and palletizing the mixture, thus obtaining the finished product. The invention has the function of oxidation resistance, can alleviate physical fatigue and strengthen immunity of human body.
WO2009156099A8 6-substituted isoquinolines and isoquinolinones The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
WO2010063011A3 Methods for the treatment of infections and tumors PD-I antagonists are disclosed that can be used to reduce the expression or activity of PD-I in a subject. An immune response specific to an infectious agent or to tumor cells can be enhanced using these PD-I antagonists in conjunction with an antigen from the infectious agent or tumor. Thus, subjects with infections, such as persistent infections can be treated using PD-I antagonists. In addition, subjects with tumors can be treated using the PD-I antagonists. In several examples, subjects can be treated by transplanting a therapeutically effective amount of activated T cells that recognize an antigen of interest and by administering a therapeutically effective amount of a PD-I antagonist. Methods are also disclosed for determining the efficacy of a PD-I antagonist in a subject administered the PD-I antagonist. In some embodiments, these methods include measuring proliferation of memory B cells in a sample from a subject administered the PD-I antagonist.
WO2014046065A1 Advanced heart failure treatment material as myocardial/cardiovascular regeneration device Provided is a material that, as a myocardial/cardiovascular regeneration device, is for the treatment of advanced heart failure, and with respect to the fundamental treatment of intractable circulatory diseases regarding which not only saving lives but also improving quality of life (QOL) are pressing issues, particularly advanced heart failure, has a high treatment effect, and by means of commercialization rendering unnecessary (cell-free) the culturing of cells by performing stem cell control, has increased universality and is self-assembled in a manner capable of emergency use. The advanced heart failure treatment material is provided with a drug, a drug holding agent, and a myocardial support device.
CN102397229A Refreshing and brain invigorating liquid shampoo The invention discloses a refreshing and brain invigorating liquid shampoo, which relates to the technical field of articles for daily use; the preparation process comprises the steps of: taking the formula medicinal materials of 3% of donkey-hide gelatin, 1% of semen cassiae, 4% of corn cervi pantotrichum, 2% of dried ginger, 3% of herba epimedii, 3% of spina date seed, 2% of radix ophiopogonis, 2% of wolfberry, 1% of Chinese date, 3% of lucid ganoderma, 2% of chrysanthemum, 1% of lily, 2% of ginkgo, 2% of angelica, 1% of salvia miltiorrhiza, 2% of Chinese yam, 3% of Chinese Magnoliavine fruit, 2% of mulberry, 3% of semen juglandis and 2% of semen sesami nigrum to be mixed with millet wine and be soaked for three times, the soaking liquid medicines of the three times are combined and mixed together uniformly, are concentrated into cream, then 5% of deep sea mineral salt, 3% of deep sea algae, 3% of rose oil, 4% of taurine, 3% of pine oil, 5% of ginseng extract and an appropriate amount of rice vinegar are added into the mixture, uniformly mixed, decolored with activated carbon, packed and sealed. The invention has the characteristics of nourishing the scalp, recovering the scalp physiological environment balance, preventing the problems of hair oil, itching and scurf, being convenient to use, refreshing, invigorating the brain, supplementing the brain nutrition through the scalp, and perfecting the brain functions.
US7659279 2-{(2S)-2-[({4-[3-Chloro-4-fluoroanilino]-7-methoxyquinazolin-5-yl}oxy)methyl]pyrrolidin-1-yl}-2-oxoethanol; epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors; breast, colorectal and head and neck cancer The invention concerns quinazoline derivatives of the formula: (I); wherein X1, Q1, Z, R1, R2, Y, a and m are as defined in the description, which are erbB tyrosine kinase inhibitors, particularly EGFR tyrosine kinase inhibitors. Also claimed are processes for their preparation; pharmaceutical compositions containing them; and their use as therapeutic agents in the treatment of erbB tyrosine kinase mediated diseases such as cancer.
US7691841 Azetidine derivatives as CCR-3 receptor antagonist Compounds of formula I in free or salt form, wherein Ar, X, Y and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
US20090186916 Aminoindane derivative or salt thereof Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3-dihydrdo-1-benzofuran, 2,3-dihydrdo-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.
WO2008101907A3 N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase Novel substituted amide inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSDl) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
EP2240472A1 2-amino-quinoline derivatives useful as inhibitors of -secretase (bace) The present invention is directed to novel 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and / or dementia. The compounds of the present invention are inhibitors of β-secretase, also known as β-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2.
CN103285081A Corrosion cleaning liquid The invention provides corrosion cleaning liquid containing chloramphenicol eye drops, compound dexamethasone acetate cream and a hydrogen peroxide bacteria-inhibiting washing agent, wherein the chloramphenicol eye drops, the compound dexamethasone acetate cream and the hydrogen peroxide bacteria-inhibiting washing agent are mixed according to a volume ratio of (90-95): (2-4): (3-6). The corrosion cleaning liquid disclosed by the invention has the characteristics of quick acting in a sterilizing and disinfecting process, good therapeutic effects, small skin irritation in a sterilizing and inflammation diminishing process, no acute pain feel; and the diseases hardly recur after being healed by using the corrosion cleaning liquid.
EP1914237A2 Phosphonate ester antiviral compounds The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g. osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
WO2012156877A8 Treating skin exposed to uv radiation with quetiapine or analogs thereof The present invention includes methods for treating sun-exposed skin, such as treating photoaging and treating skin cancer. Also included are methods for altering a cell's response to ultraviolet radiation. The methods include administration of quetiapine or an analog thereof or a pharmaceutically acceptable salt, solvate, or prodrug thereof.
US20100120873 Prophylactic or therapeutic agent for age-related macular degeneration An object of the present invention is to find a novel medicinal use of 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof. 2-Phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof exhibits an excellent inhibitory effect on neovascularization in the choroid and also has a protective effect on retinal pigment epithelial cell damage, and therefore is useful as a prophylactic or therapeutic agent for age-related macular degeneration.
CN100594795C Fat and oil composition Provided is a fat or oil composition containing the following components (A), (B) and (C): (A) 100 parts by weight of a fat or oil containing from 0.1 to 10 wt.% of a monoglycerol monofatty acid ester, from 1 to 64.9 wt.% of a monoglycerol trifatty acid ester, and from 35 to 98.9 wt.% of a monoglycerol difatty acid ester having an unsaturated fatty acid content, in fatty acid components, of from 80 to 100 wt.%; (B) from 0.1 to 3.0 parts by weight of a diglycerol fatty acid ester containing from 40 to 100% of a difatty acid ester having an unsaturated fatty acid content, in the fatty acid components, of from 70 to 100 wt.%; and (C) from 0.01 to 2 parts by weight of an antioxidant.
CN101190218B New use of tizanidine and its derivatives in preparing medicine for treating anxiety disorder The invention relates to a novel application of both tizanidine and a ramification of tizanidine, in particular to the novel application of both tizanidine and the tizanidine ramification in the process of preparing medicines used for treating anxiety disorder. The invention also provides an application of a medicine compound containing tizanidine and the tizanidine ramification in the process ofpreparing medicines used for treating anxiety disorder. As a central muscle relaxants pain-releasing medicine, tizanidine not only can release the pain but also can solve the anxiety of pain sufferers.
US20110129466 Methods of treating cancer by administering antibodies to cd200 Methods and compositions for regulating immunity are disclosed. For enhancing an immune response, agents that inhibit OX-2 are administered. Such methods are useful in treating cancer. For suppressing an immune response, an OX-2 protein or a nucleic acid encoding an OX-2 protein is administered. Such methods are useful in preventing graft rejection, fetal loss, autoimmune disease, allergies and in inducing tumor cell growth.
WO2009009531A2 Pyrimidinecarboxamide derivatives for the treatment of hiv infections This disclosure relates to novel HTV integrase inhibitors their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating HTV infections. Formula I: or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein: each of R1, R2a, R2b, and R3 is independently selected from CH3, CDH2, CD2H, and CD3; Y1 and Y2 are each independently selected from H or D; R4 is selected from: formula D:and D; and when each R is CH3, at least one Y is D.
CN101091702A Oral disintegration tablet of Bromhexine Hydrochloride The present invention relates to a new bromhexine hydrochloride oral disintegrating tablet. Its preparation method includes the following steps: melting, hot extrusion, cooling, granulating and tabletting.
CN103462909A Formulation of nizatidine for injection and preparation technology thereof The invention provides nizatidine for injection, which is simple in assistant, safe to use in medicine, and high in stability. According to the nizatidine for injection disclosed by the invention, the selected assistant is mannitol, wherein the mass ratio of a main drug nizatidine to the assistant mannitol is 2:1. The nizatidine for injection disclosed by the invention has the stability according with the requirements within a pH range from 6.0 to 7.5, preferably the pH range is 6.8-7.2. The nizatidine for injection disclosed by the invention can be prepared into an injection form, also can be prepared into a freeze-dried powder preparation form, and has good stability.
WO2012127277A3 Bendamustine anionic-catioinic cyclopolysaccharide compositions The present invention is directed to pharmaceutical compositions including: (a) bendamustine, (b) a first charged cyclopolysaccharide, and (c) a stabilizing agent which is a second charged cyclopolysaccharide having a charge opposite to that of the first charged cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. The compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
US20060074053 Ophthalmic solution containing quinolone antimicrobial compound The present invention provides an ophthalmic solution containing as the active ingredient a quinolone antimicrobial compound, wherein at least one member selected from the group consisting of water-soluble vinyl polymeric compounds and water-soluble cellulose derivatives is formulated into the ophthalmic solution to prevent the quinolone antimicrobial compound from precipitating when the ophthalmic solution comes in contact with the lacrimal fluid after instillation.
US20080095854 Ballast administering to mammals skins; high density core overcoated with amorphous reservoir containing dna; drug delivery; containing free radical scavenger The present invention relates to DNA formulations suitable for ballistic delivery into the skin of the human body. In particular the present invention provides DNA formulations suitable for ballistic administration of DNA vaccines into the skin. The present invention provides a novel DNA pharmaceutical agent dosage form, having a dense core element which is coated with an amorphous solid reservoir medium containing the DNA pharmaceutical agent.
EP1390491B1 Method for treating neurodegenerative, psychiatric and other disorders with deacetylase inhibitors The invention relates to a novel method for treating a variety of diseases and disorders, including polyglutamine expansion diseases such as Huntington's disease, neurological degeneration, psychiatric disorders, and protein aggregation disorders and diseases, comprising administering to patients in need thereof of a therapeutically effective amount of one or more deacetylase inhibitors. The invention is also directed to a transgenic fly useful as a model of polyglutamine expansion diseases, which may be used to test potential therapeutic agents.
CN102048700A Colon targeted preparation of semi-pinnated brake herb extract 5F and preparation method thereof The invention discloses a colon targeted preparation of semi-pinnated brake herb extract 5F and a preparation method thereof. The preparation is an oral preparation which is prepared by coating the semi-pinnated brake herb extract 5F-containing pellets by adopting colon targeted coating liquid or directly filling the semi-pinnated brake herb extract 5F-containing pellets into colon targeted capsule shells, and is released at a colon site. After being taken orally, the preparation is not released in the stomach and the small intestine and is started to release after reaching the colon site to increase the medicament concentration of a colon diseased part locally, thereby contributing to the treatment of colitis and colon cancer, reducing medicament dosage and reducing toxic and side effects generated by medicament metabolism in the liver.
EP1406910B1 Preparation methods of derivatives of bisphosphonates The invention concerns novel salified or partly esterified 1-hydroxymethylene-1,1-bisphosphonic acid derivatives, pharmaceutical compositions comprising same, their therapeutic use, in particular for treating cancer tumours. The invention also concerns methods for preparing said derivatives.
WO2007054197A1 Food products, ingredients therefor and use of those food products and ingredients A food composition comprises at least one of protein and carbohydrate, The composition further comprises 0.3-35 wt.% of an organogel comprising an edible oil, a phytosterol and a phenolic acid ester of a phytosterol. It may be used for promoting satiety and/or other health benefits.
EP2473046A1 Iminosugars and methods of treating filoviral diseases Provided are methods of treating a disease or condition caused by or associated with a virus belonging to the Filoviridae family using iminosugars, such as DNJ derivatives.
CN1617733B Method of treatment of gastrointestinal disease and polymeric composition for use therein A method of treatment of gastrointestinal disease by administering polymeric antimicrobial comprising a derivative of poly(2-propenal, 2-propenoic acid) formed by reaction between a poly(2-propenal, 2-propenoic acid) and an alcohol or phenol to form protected carbonyl groups. The invention also relates to composition for use in treatment of gastrointestinal disease.
DE102008000351A1 Preparing ebastine containing granules, useful to treat e.g. allergic rhinitis, comprises preparing granules from a solution of ebastine in cyclic ether solvent and a powder of one or more existing solid carrier materials, and drying Preparing ebastine containing granules, comprises: (a) providing a solution of ebastine in one or more cyclic ether solvents; (b) preparing granules from the obtained solution and a powder of one or more existing solid carrier materials; and (c) drying. Independent claims are included for: (1) a process for preparing a solid pharmaceutical composition containing ebastine, comprising preparing the granules and molding in a conventional manner into tablets or capsules; (2) the granules containing ebastine obtained by the process; and (3) the solid ebastine containing the composition. - ACTIVITY : Antiallergic; Antiinflammatory; Ophthalmological; Antipruritic; Dermatological. - MECHANISM OF ACTION : Histamine 1 (H1) receptor antagonist.
CN101390873A Cytidine disodium triphosphate and arginine composition and preparation method thereof The invention relates to a combination of cytidine disodium triphosphate and arginine, and the preparation method thereof; the freeze-dried powder adopts arginine as the pH regulator, has good stability, long storage time, and no local irritation and pain.
CN101167719B Gallo catechin and gallate microcapsule granule and preparation technique thereof The invention relates to pigallocatechin gallate (EGCG) microcapsule granules and a process for preparation. The microcapsule granules take pigallocatechin gallate as the capsule core, cellulose ethylether (EC) and or carbowax (PEG) as the capsule body, and sodium carboxymethylstarch (CMS-Na) as the accelerating agent. The microcapsule granules have the advantages of good stability, excellent effect, and stable dissolution rate, and resolve the problems of absorbent quality and flowability of pigallocatechin gallate. The invention is applicable for the development of medicament, food, feed stuff and the like.
US20070232628 Calcium receptor antagonists; 2-(2-hydroxy-phenyl)-3-(4-isopropyl-phenyl)-5,6,7,8-tetrahydro-3H-quinazolin-4-one; bone disorders; hypoparathyroidism, osteosarcoma, periodontal disease, fracture healing, osteoarthritis, rheumatoid arthritis, Paget's disease, humoral hypercalcemia, osteoporosis Novel calcilytic compounds and methods of using them are provided.
US20100113386 N-benzyl substituted pyridyl porphyrin compounds and methods of use thereof The present invention relates to N-Benzyl-Substituted Pyridyl Porphyrin Compounds, compositions comprising an effective amount of an N-Benzyl-Substituted Pyridyl Porphyrin Compound and methods for treating or preventing injury due to exposure to a reactive species, erectile dysfunction, urinary incontinence, lung disease, hyperoxia, neurodegenerative disease, liver disease, myocardial damage during cardioplegia, an inflammatory condition, a reperfusion injury, an ischemic condition, a cardiovascular disease, diabetes, a diabetic complication, cancer, a side effect of cancer chemotherapy, or a radiation-induced injury, and methods for prolonging the half-life of an oxidation-prone compound, comprising administering to a subject in need thereof an effective amount of an N-Benzyl-Substituted Pyridyl Porphyrin Compound.
CN101258159A Novel c18 modified retrosteroids as progesterone receptor modulator compounds Described herein are new retrosteroidal compounds of general formula (I), representing progesterone receptor modulators, and their production, and pharmaceutical preparations containing these compounds. Said compounds are preferably used for the treatment of benign gynecological disorders such as endometriosis and uterine fibroids, as well as for female birth control and for HRT.
CN1682756A Supplementing method for exogenous nitric oxide The method of supplementing exogenous NO is to sealing NO in edible encapsulant, such as gelatin encapsulant to form stable, convenient and safe NO capsule. The exogenous NO is supplemented into body via oral taking to produce the effects of lowering blood pressure, raising body's anoxia and fatigue resistance, preventing and treating cerebral edema, pulmonary edema, apoplexy, cardiac and cerebral vascular diseases and other NO relevant diseases.
WO2007079928A1 Substituted oxazole derivatives with an analgesic action The invention relates to substituted oxazole derivatives of formula (I), to a method for their production, to medicaments containing said compounds and to the use of substituted oxazole derivatives for producing medicaments.
CN101675916A Preparation method of levo-ofloxacin hyaluronic acid gel slow-released agent The invention provides a preparation method of a levo-ofloxacin hyaluronic acid gel slow-released agent. The preparation, which contains hyaluronic acid and levo-ofloxacin, is prepared in the way thatthe hyaluronic acid is dissolved at higher temperature and then the levo-ofloxacin is added. The levo-ofloxacin hyaluronic acid gel slow-released agent of the invention has good biological compatibility and longer half-life, and is suitable for antibiosis and antiphlogosis under various conditions.
US20080108629 Heterocyclic Derivatives for the Treatment of Diseases Mediated by Stearoyl-Coa Desaturase Enzymes Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
EP1069894B1 Spisulosine compounds having antitumour activity Investigation of the activity of extracts of the clam Spisula polynyma has led to antitumour long-chain, straight-chain alkane or alkene compounds which have a 2-amino group and a 3-hydroxy group.
WO2009095712A3 4-(3-amin0pyraz0le) pyrimidine derivatives for use as jak kinase inhibitors in the treatment of cancer The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.
WO2012154774A1 Combinations of solifenacin and salivary stimulants for the treatment of overactive bladder Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release solifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release solifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of alleviating a side effect of treatment for overactive bladder in a patient suffering therefrom, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release solifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.
CN102188547A Detoxification particle containing isatis root and coptis chinensis and preparation method thereof The invention discloses a detoxification particle containing isatis root and coptis chinensis and a preparation method thereof. The medicament is prepared from, in a certain weight ratio, isatis root, coptis chinensis, folium isatidis, Chinese pulsatilla root, artemisia capillaries, banksia rose, licorice and borneol. The medicament of the invention has the efficacies of clearing heat and detoxifying, cooling blood, expelling phlegm and arresting coughing, astringing intestine and relieving dysentery, discharging fire, eliminating dampness, detoxifying, killing parasites, antibiosis and antiphlogosis, anti-virus, promoting qi circulation and relieving pain, warming middle energizer to regulate stomach, warming kidney and enhancing yang, replenishing qi to invigorate the spleen, promoting diuresis, dispelling damp, warming middle energizer to dispel cold and warming middle energizer to regulate water. In addition, the medicament has a short treatment course, substantial curative effect, low costs, high cure rate and non-recurrence. Therefore, the medicament can be applied to treat common diseases of livestock and poultry, such as cold and heating, cough and asthma, sore throat, damp-heat diarrhea, heat stress and heatstroke.
WO2014142995A1 Compositions and methods including leelamine and arachidonyl trifluoromethyl ketone relating to treatment of cancer The present invention relates to compositions and methods for treatment of proliferative disease. In specific aspects, the present invention relates to compositions including (1 R,4aS, 10aR)- 1,2,3,4,4a,9, 10, 10a-octahydro- 1 -,4a-dimethyl-7-( 1 - methylethyl)-1-phenanthrenemethanamine (leelamine) and arachidonyl trifluoromethyl ketone (ATK) in combination; methods for treatment of cancer including administration of leelamine and ATK in a subject in need thereof; and particularly methods for treatment of skin cancer including administration of leelamine and ATK in a subject in need thereof.
CN102743375A Use and drug composition of isoorientin The invention discloses a use and a drug composition of isoorientin. The isoorientin has a significant inflammation inhibition effect, and can form a novel potential anti-inflammation drug so as to provide an application. In anti-inflammation drugs, the isoorientin is adopted as an anti-inflammation active component, and the isoorientin and pharmaceutically-acceptable excipients and/or medicinal carriers are prepared into various medicinal formations by adopting a conventional method.
CN101422474A Use of magnesium isoglycyrrhizinate preparation for vein in treating skin disease The invention belongs to the field of medical preparation, in particular to the application of a magnesium isoglycyrrhetate preparation used in veins for preparing a medicament for curing psoriasis, the application for preparing the medicament for curing chronic eczema dermatitis, the application for preparing the medicament for curing dermatitis contacta as well as the application for preparing the medicament for curing other abnormality dermatosises except the diseases. The invention is characterized in that the weight-volume ratio of the content range of the magnesium isoglycyrrhetate in the preparation is 0.01 to 10 percent and the PH value range is 6.5 to 8.
WO2011158149A1 2-(3,5-disubstitutedphenyl)pyrimidin-4(3h)-one derivatives O N NH R3 R2 O R1 168 ABSTRACT The present invention provides a 2-(3,5-disubstitutedphenyl)pyrimidin- 4(3H)-one compound of Formula (I) 5 (I) or a pharmaceutically acceptable salt thereof wherein R 1, R2 and R3 are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and 10 the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.
WO2008089268A3 Methods and compositions for treating conditions associated with infection and/or inflammation The present invention provides methods and compositions for treating and preventing conditions characterized by infection and/or inflammation, especially of the eyes, ears, nose, and/or throat. The methods of the invention involve administering hypohalous acid to the patient, such as in the form of a composition described herein.
CN103735524A Cefixime chewable tablet and preparation method thereof The invention discloses a cefixime chewable tablet and a preparation method thereof. The method comprises the following steps: (1) screening cefixime through a 100-mesh screen, and respectively screening mannitol, a disintegrating agent, an adhesive, orange flavor and a lubricant for later use; (2) adding the cefixime, a sweetening agent, a disintegrating agent, an adhesive and a flavoring agent into a mixer, and uniformly mixing to obtain medicinal powder; and (3) adding magnesium stearate into the medicinal powder obtained in the step (2), uniformly mixing, and preparing the cefixime chewable tablet by adopting a method of directly tabletting powder. The cefixime chewable tablet disclosed by the method is good in taste and stable in quality, and the effective components of the medicine can be quickly absorbed through mouth mucosa by virtue of chewing. The cefixime chewable tablet is quick in absorption, high in bioavailability and remarkable in curative effect, and can solve the problems in the prior art.
CN102688229A Application of epicatechin as drug for raising leucocytes The invention discloses an application of epicatechin as shown in the formula (I) in preparation of products for preventing or treating leucocytopenia. The leucocytopenia can be caused by antipyretic analgesics, antibiotic, antipsychotics, antithyroid agents, anticarcinogen or radiotherapy. Preferred antipyretic analgesics are selected from amidopyrine, analgin or compound aspirin. Preferred antibiotic is selected from chloramphenicol, penicillin or sulfonamide. Preferred antipsychotics are selected from chlorpromazine, perphenazine and trifluoperazine. Preferred antithyroid agents are selected from propylthiouracil and tapazole. Preferred anticarcinogen is selected from cyclophosphamide. The product is selected from a medicine, a health product or a foodstuff.
US8404674 Substituted 9H-purin-2-YL compounds, compositions thereof and uses thereof The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
CN101491508B Preparation method of aspirin Intestine-soluble micro-pill capsules The invention relates to a method for preparing an aspirin enteric-coated micro-pill capsule. The method comprises that: the method selects 50 to 80g of aspirin with 0 to 300 microns, uses 1 to 5g of povidone and 0.1 to 0.8g of hydroxypropyl methylcellulose and uses 5 percent ethanol solution in percentage by mass as a wetting agent to prepare an active pill core; the method selects 3 to 60g of acoating auxiliary material with enteric-coated function, 0.3 to 6g of a plasticizer, 0.01 to 0.06g of a releasing agent, 0.1 to 0.5g of talcum powder and 5 to 30g of purified water to prepare a solution for coating; and a micro-pill is directly filled to prepare the aspirin enteric-coated micro-pill capsule. The preparation method is simple, low in cost, beneficial for environment and favorable for industrialized production; and the prepared aspirin capsule has good stability and obviously reduces generation of side effect.
CN103222980A Environment-friendly chick immunopotentiator The invention relates to an environment-friendly chick immunopotentiator. The environment-friendly chick immunopotentiator is prepared by mixing morida officinalis how polysaccharide, gamma-aminobutyric acid, arginine, taurine and lysine uniformly, wherein the morida officinalis how polysaccharide is prepared by extracting morida officinalis rootstock by the conventional water extraction and alcohol precipitation method. The environment-friendly chick immunopotentiator has a simple preparation process, scientifically combines South China medicine morida officinalis how polysaccharide and amino acid such as GABA, effectively promotes improvement of the growth performance and the immune function of the chicks and enhances the immune function of the chicks; the immunization time is long; the preparation is simple in composition; the materials are easy to obtain; various components belong to safety components; the problems of medicine residues, toxic or side effect and the like are avoided; and the environment-friendly chick immunopotentiator is environment-friendly, efficient and stable.
WO2010098495A1 Imidazolylpyrazine derivatives To provide a novel low-molecular-weight compound that inhibits the production of amyloid-β (Aβ ). A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein R1 and R2 are the same or different and each represent a substituent selected from the following Substituent Group a1; m represents an integer of 0 to 3; n represents an integer of 0 to 2; X1 represents a single bond or the like; X2 represents a single bond or the like; Ring A represents a five-membered aromatic heterocyclic group or the like which contains two or more nitrogen atoms and may have 1 to 3 substituents selected from the following Substituent Group b1; and Ring B represents a monocyclic or fused cyclic aromatic ring group such as the formula [2] which may have 1 to 3 substituents selected from the following Substituent Group c1, is effective as a therapeutic agent for a disease such as Alzheimer's disease. Substituent Group a1: a C1-6 alkyl group and the like Substituent Group b1: a C1-6 alkyl group and the like Substituent Group c1: an amino group and the like
WO2008061447A1 A medicine for treating eczema and process of ointment thereof A medicine for treating eczema and process of ointment thereof. The medicine is prepared by using 150-600 parts by weight of radix sophora flavescens Ait., 100-300 parts by weight of cortex dictamnus dasycarpus Turcz., 150-600 parts by weight of cortex paeonia suffruticosa Andr., and 5-25 parts by weight of borneol as raw materials.
US20120190652 Diagnostic agent for parkinson's disease The present invention relates to method of identifying whether or not an individual has Parkinson's disease (PD). In particular, the invention relates to a method for identifying whether or not an individual has PD in the pre-symptomatic phase of the disease or to distinguishing PD from another neurological disorder. The method of the invention comprises measuring the amount of soluble α-synuclein oligomers in a cerebrospinal fluid sample taken from an individual. The method optionally also comprises measuring the total amount of α-synuclein in the CSF sample, calculating the ratio of the amount of α-synuclein oligomers to the total amount of α-synuclein, and thereby determining whether or not the individual has PD. The method of the invention can be used in clinical trials to measure the effect of drugs in both PD animal models and human PD patients.
CN101953800A Technology for producing water-soluble coenzyme Q10 and mannitol composite powder The invention discloses technology for producing water-soluble coenzyme Q10 and mannitol composite powder, which is characterized by comprising the following steps of: modifying the grain size of mannitol, screening, and uniformly mixing with coenzyme Q10 according to the preset ratio; making the crystalline nature of the coenzyme Q10 in the mixed powder change under the condition of a certain temperature and forming a coenzyme Q10 and mannitol complex, and reducing the complex to a certain temperature so as to improve the hardness; and modifying the grain size of the complex and screening, namely the prepared powder is the water-soluble coenzyme Q10 and mannitol composite powder. The prepared coenzyme Q10 composite powder has the advantages of high water solubility, high yield, low cost and easy industrialization.
US20120046322 Bioavailable Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
CN102633817A Cefoxitin esterified prodrug compound and oral preparations The invention discloses an esterified prodrug compound and salt forming compounds and oral preparations thereof. The prodrug compound is shown in the structural formula (IV) in the specification, takes cefoxitin as an active ingredient and can exist in the form of salts. The prodrug compound has the following advantages that a lipophilic group acetoxy-1-halothane is introduced on the basis of cefoxitin to esterify carboxyl to become the esterified prodrug, thus providing an active pharmaceutical ingredient changing the original dosage forms; orally taken, the esterified prodrug not only relieves pains suffered by the patients during injection but also is not only used in professional organizations, thus saving time and widening the application range of the drug; and the esterified prodrug has a confirmed curative effect.
WO2013106812A1 Personalized medicine for the prediction of therapy targeting the hedgehog pathway Methods and composition for tumor therapy, especially esophageal adenocarcinoma (EAC), are described. For example, in certain aspects methods for determining Hedgehog and mTOR signaling pathway status to select patients for administering a combination therapy of Hedgehog and mTOR signaling inhibitors are described. Furthermore, the invention provides compositions that involve testing kits for determining signaling status.
CN102743401A Application of panaxadiol saponins fraction in preparing medicine for preventing epilepsia The invention provides application of a panaxadiol saponins fraction in preparing a medicine for preventing epilepsia. The component comprises the following main constituents: ginsenoside Rb1, ginsenoside Rb2, ginsenoside Rb3, ginsenoside Rc and ginsenoside Rd, and the medicine is prepared from active constituents in the single panaxadiol saponins fraction or from the active constituents in the single panaxadiol saponins fraction and other medicines. By taking one of five panaxadiol saponins: ginseng, American ginseng rhizome medicinal materials, ginseng stems and leaves, American ginseng stem and leaf medicinal materials and total extractives or total saponins of the ginseng, the American ginseng rhizome medicinal materials, the ginseng stems and leaves and American ginseng stem and leaf medicinal materials as a starting raw material independently or taking a mixture which consists of two or more than two different raw materials as the starting raw material comprehensively, the medicine is prepared by establishing the chromatographic separation and purification technology. According to the medicine prepared from the panaxadiol saponins fraction provided by the invention, an anti-epileptic effect can be greatly improved, and moreover, the toxic and side effects, especially dermatitis and intelligence toxicity, of traditional anti-epileptic medicines can be resisted, therefore, long-standing defects that the anti-epileptic medicines are not enough in curative effect and low in safety are overcome. The structural formula of the panaxadiol saponin is shown in specification.
CN102988454A Compound preparation for treating anal fissure The invention relates to a compound preparation for treating anal fissure. The preparation comprises the following raw materials in parts by weight respectively: 50 to 200 parts of talcum powder, 60 to 300 parts of calaminem, 80 to 600 parts of frankincense, 50 to 600 parts of myrrh, 10 to 60 parts of red upborne elixir; and Vaseline is served as an auxiliary material. The preparation method of the preparation comprises the following steps: step 1); weighing talcum powder, calaminem, frankincense, myrrh and red upborne elixir, respectively preparing into powder and mixing, or preparing into powder after mixing together, and then obtaining the mixed powder; and step 2); weighing the mixed powder obtained in the step 1), and fully mixing with vaseline which is served as the auxiliary material, wherein the weight ratios of the mixed powder and vaseline are as follows: the mixed powder takes up 15% of total weight, and vaseline takes up 85% of total weight. The compound preparation for treating anal fissure has the efficacies of promoting qi circulation and relieving pain, eliminating swelling and promoting tissue regeneration and stopping itching and healing sore, and can be used for treating various anal fissures. Furthermore, proved by clinical cases, the compound preparation for treating anal fissure can effectively treat various anal fissures and has a more satisfactory ideal effect by cooperating with the surgical treatment.
WO2012028732A1 Novel uses of v-atpase inhibitors Benzolactone v-ATPase inhibitors for use in the treatment of influenza A virus infections are described. The compounds are administered in therapeutically-effective, sub-cytotoxic amounts. Methods for the treatment of influenza A infections using benzolactone v-ATPase inhibitors are also described.
CN103735922A Medicine for treating trachoma and preparation method thereof The invention discloses a medicine for treating trachoma and a preparation method thereof. The medicine comprises the following components according to a certain weight ratio: dried orange peels, radix paeoniae rubra, fructus forsythia, radix sileris, rhizoma anemarrhenae, natrii sulfas exsiccatus, cortex Dictamni and the like. The medicine of the invention has the functions of clearing heat and cooling blood, eliminating stasis and relieving pain, promoting the production of body fluid and improving eyesight, and operates quickly and has good curative effect in treating trachoma, and the disease does not recur after cure.
WO2009153566A1 Cyp26 inhibitors A compound of formula (I) wherein X is selected from O, S, NH or CH2; Rd and Rp are optional naphthyl group substituents; RHet is imidazolyl, triazolyl or pyridyl; and Rc is C1-4 alkyl substituted by a group selected from: hydroxy, amino, amido, carboxy, C1-7 alkyl ester, C5-7 aryl-C1-2 alkyl ester, sulfonamino, sulfinamino, hydroxamino and tetrazolyl.
US7112337 Liposome mixture of a lipid that is neutral in charge at physiologic pH and positively charged at pH values less than physiological pH, and a lipid joined to a hydrophilic polymer by an aromatic disulfide linkage, associated with a nucleic A liposome composition for delivery of a nucleic acid in vivo or ex vivo is described. The liposomes in the composition are comprised of (i) a lipid that is neutral in charge at physiologic pH and positively charged at pH values less than physiologic pH and (ii) a lipid joined to a hydrophilic polymer by a dithiobenzyl linkage. The liposomes are associated with a nucleic acid for delivery to a cell.
US20070270394 Sex steroid precursor alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 cGMP phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausal women Novel methods for treating or reducing the likelihood of acquiring vaginal dysfunctions, more particularly vaginal dryness and dyspareunia, leading to sexual dysfunction and low sexual desire and performance , in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor. Further administration of estrogen or selective estrogen receptor modulator, particularly those selected from the group consisting of Raloxifene, Arzoxifene, Tamoxifen, Droloxifene, Toremifene, Iodoxifene, GW 5638, TSE-424, ERA-923, and lasofoxifene, and more particularly compounds having the general structure: is specifically disclosed for the medical treatment and/or inhibition of development of some of these above-mentioned diseases. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
CA2327395C New imidazotriazolopyrimidines, processes for preparing them and their use as pharmaceutical compositions The invention relates to new imidazotriazolopyrimidine derivatives of general formula (I), processes for preparing them and their use as pharmaceutical compositions wherein the dotted lines between the nitrogen atoms indicate the existence of a double bond in one of two possible positions, so that the groups R4 and R6 and R3 and R2 need not be present simultaneously and wherein the groups R1 to R6 may have the meanings given in the specification and claims.
US20120302614 Method for improving cerebral circulation or treating a cerebral blood flow disorder A method for improving cerebral circulation or treating a cerebral blood flow disorder, comprising administering a pharmacologically effective amount of an angiotensin II receptor blocker to a human.
CN101711740A Method for preparing targeted curcumin nanoparticles for treating ulcerative colitis The invention discloses a prescription of targeted curcumin-polylactic acid-hydroxyacetic acid copolymer (PLGA) nanoparticles for treating ulcerative colitis and a preparation process thereof. The prescription uses the targeting characteristic of the nanoparticles to an inflammatory part to reduce a medicament administration dosage and side effect and improve treatment effect. The preparation process comprises the following steps: taking a biodegradable material PLGA as a carrier material, polyvinyl alcohol as an emulsifier and 2 to 5 percent cane sugar as a freeze-drying protective agent, adding PEG 6000 into a water phase, and preparing the curcumin-PLGA nanoparticles by an emulsion-solvent volatilization method. The prescription process is optimized by taking the grain sizes of the nanoparticles and a medicament-loading rate as indexes. The prepared nanoparticles are round or elliptic and uniform in the size, have a mean grain size of 20 to 800nm and the medicament-loading rate of 10 to 20 percent, reduce dumping effect and have obviously better treatment effect on an animal pattern than a 5-aminosalicylic acid control group.
WO2007009723A3 Azepane- or azocane-substituted pyrazoline derivatives, their preparation and use as medicaments The present invention relates to Azepane- or Azocane- substituted substituted pyrazoline compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals
CA2402446C 1,8-naphthalimide imidazo[4,5,1-de]acridones with anti-tumor activity The invention provides imidazoacridone compounds of general formula (1) which have cytotoxic and anti-tumor activity. The invention also provides methods of preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.
US20070232564 Fish-Origin Chondroitin Sulfate/Dermatan Sulfate Hybrid Chain It is intended to provide a novel chondroitin sulfate/dermatan sulfate hybrid chain having biding activity toward a variety of growth factors, neurite outgrowth-promoting activity, and anticoagulant activity and to provide a composition for neurological disease treatment. The novel chondroitin sulfate/dermatan sulfate hybrid chain was separated and purified from the bodies of fishes other than bony fishes. When shark skin is used, the hybrid chain comprises a disaccharide GlcUA(2S)-GalNAc(4S) and has an average molecular weight of 65 to 75 kDa, and the degree of sulfation per disaccharide molecule falls within the range of 0.7 or more to less than 1.20. The hybrid chain is capable of binding to a variety of growth factors and further possesses neurite outgrowth-promoting activity and anticoagulant activity.
US20100076010 Alpha 1a-adrenoceptor antagonists This invention relates to novel compounds that are dihydroindoles derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel dihydroindoles derivatives that are derivatives of silodosin. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an α-1A-adrenoreceptor antagonist, such as silodosin.
WO2012153076A2 Cosmetic skin treatment method comprising two successive steps The invention relates to a method for the cosmetic treatment of the skin and/or mucous membranes, consisting in successively applying two cosmetic compositions to the skin and/or mucous membranes, namely: a first composition containing a single active ingredient that can correct a skin dysfunction, optionally in the presence of a pro-penetrator system; and, immediately following the application of the first composition, a second composition which, depending on skin type, has a nourishing and/or hydrating and/or protective action and/or enhances complexion radiance and/or elasticity and/or matt appearance.
US7741346 Vision defects; anticancer agents; antitumor agents An object of the present invention is to find new pharmacological actions of urea compounds having structure represented by the general formula [1]. The urea compounds having the structure represented by the general formula [1] have excellent angiogenesis inhibitory actions. [wherein “A” is —(NR4)—, —(CR5R6)— or —O—, “B” is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantylalkyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfur].
WO2014100834A1 Methods and compositions for treatment of cyanide and hydrogen sulfide toxicity A composition and method for treating excess cyanide and hydrogen sulfide comprising administering a cobinamide. Further a method for determining extent of binding by an agent to an extracellular matrix.
EP2283835A2 Method and preparation for treating metabolic stress The invention is concerned with a method and a composition for treating or preventing catabolism or of stimulating anabolism in a mammal undergoing metabolic stress. The method comprises administering to the mammal a composition containing methyl donors selected from the group consisting of L-serine, methionine, choline, phosphatidyl choline, betaine, dimethylglycine, sarcosine, methylated folates, S-adenosyl methionine, thymidine triphosphate, adenosine triphosphate and optionally methyl acceptors selected from the group consisting of L-glycine, ethanolamine, phosphatidyl ethanolamine, folate, ribose, wherein the total molar amount of methyl donors delivered by the method exceeds the total molar amount of methyl acceptors delivered by the method by at least 0.18 mmol per kg of body weight per day.
WO2011119126A1 Use of oxalic acid in the production of a therapeutic preparation with anti-tumour activity in relation to malignant cells, a therapeutic preparation based thereon and a method of treatment The invention relates to medicine, in particular to means for the treatment of oncological diseases and may be used as the basis for creation of therapeutic preparations. Oxalic acid is used in the production of a therapeutic preparation which exhibits anti-tumour activity in relation to malignant cells. A therapeutic preparation contains oxalic acid as an organic acid, and lithium chloride as a chloride, and additionally contains dimethylxanthine, fluorouracil and sodium thiosulphate with the following ratio of all components (wt.%): oxalic acid 0.2-3.2, lithium chloride 0.2-3.1, dimethylxanthine 0.1-1.8, fluorouracil 0.1-1.8, sodium thiosulphate 0.2-3.1, distilled water to 100. A method for treatment of malignant tumours comprises taking the therapeutic preparation internally, for which purpose 5 ml of the therapeutic preparation is diluted in 50-100 ml of water, it is taken perorally once daily during a three-month course, the condition of the patient is checked monthly and a decision on whether to continue the course of treatment or to terminate it is taken on the basis of the results of cytological analyses; the treatment is repeated every 2-3 years.
WO2007130075A1 Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
CN103565801A Composition for treating fundus macular oedema and application of composition to treating eye diseases The invention discloses a composition for treating fundus macular oedema and application of the composition in treatment of eye diseases and belongs to the technical field of medicines. The composition for treating the fundus macular oedema comprises the following components in percentage by weight: 0.4-71% of (a) polyphenolic compounds, 0.6-93% of (b) lipoic acid, dihydrolipoic acid, lipoic acid salt or lipoamide, 0-97% of (c) ubiquinone or panthenol and 0-87% of (d) docosahexaenoic acid or ethyl ester thereof and/or timnodonic acid or ethyl ester thereof. The composition can be used for improving patient visual acuity, stabilizing intraocular pressure and reducing various ocular inflammations such as the fundus macular oedema. By means of the composition for treating the fundus macular oedema and a treatment method, the fundus macular oedema can be prevented, stabilized, controlled or treated and the fundus health can be enhanced; in the meantime, the intraocular pressure can be stabilized, the vision can be maintained or improved, various eye diseases or macular oedema and inflammation which are caused by eye operations can be reduced; the diabetic complication is also treated, the blood microcirculation is promoted and the liver function is improved.
WO2009058005A3 Unit dosage for brain health The invention pertains to a composition comprising (i) uridine in nucleobase, nucleoside and/or nucleotide form; (ii) docosahexaenoic acid (DHA) and/or eicosapentaenoic acid (EPA); and (iii) a tocopherol and/or an equivalent thereof, wherein said composition has: a) a weight of 200-3000 mg per unit dose; b) an energy content of less than 50 kcal per unit dose; and/or c) a volume between 0.1 and 10 ml per unit dose.The invention also pertains to the use of such composition in reducing abeta plaque burden and neurodegeneration, in the treatment of diseases related with imparted nerve functioning, in particular dementia, Alzheimer's disease and memory disorders.
CN101068826A Potent LNA oligonucleotides for the inhibition of HIF-1A expression The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5'-(T x GxGxcsasasasgscsastscscsTXGX T-3' and 5'-(G X )TXTXascstsgscscststscsTXTX A- 3', wherein capital letters designate a beta-D-oxy-LNA nucleotide analogue, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analogue or a 2-deoxynucleotide, subscript''s'' designates a phosphorothioate link between neighbouring nucleotides/LNA nucleotide analogues, and subscript''x'' designates either a phosphorothioate link or a phosphorodiester link between neighbouring nucleotides/LNA nucleotide analogues, and wherein the sequence is optionally extended by up to five 2-deoxynucleotide units. The LNA oligonucleotides are useful for modulating the expression of hypoxia-inducible factor-la (HIF-1a), e.g. in t he treatment of cancer diseases, inhibiting angiogenesis, inducing apoptosis, preventing cellular proliferation, or treating an angiogenic disease, e.g. diabetic retinopathy, macular degeneration (ARMD), psoriasis, rheumatoid arthritis and other inflammatory diseases.
EP1299089B1 Drug delivery system for poorly water soluble drugs The present invention relates to a method for modifying the solubilization rates of poorly water soluble drugs, using a chitosan-xanthan hydrogel. In addition, the present invention relates to a process for the preparation of chitosan-xanthane hydrogels as well as for the preparation of hydrogels comprising a poorly water soluble drug.
CN103735557A Application of Ilexsaponin A1 in preparation of anti-tumor medicament The invention discloses novel medicinal application of a monomer component, namely, Ilexsaponin A1 derived from plants such as ilex hainanensis in the anti-tumor aspect, namely, application of the Ilexsaponin A1 in preparation of a medicament or health-care food for treating and preventing tumors. Meanwhile, the invention further discloses dosage forms such as capsules, tablets, drop pills and injections prepared by taking the Ilexsaponin A1 as raw materials. As proved by in-vitro experiments, the Ilexsaponin A1 has a very strong inhibiting function on various tumor cell lines. Thus, the Ilexsaponin A1 can be prepared into the anti-tumor medicament and a medicament or health-care food for preventing tumors.
WO2008117790A1 Food/beverage and pharmaceutical composition for oral administration for improvement in acidic urine each comprising fucoidan as active ingredient Disclosed is a food/beverage or a pharmaceutical composition for oral administration for improving an acidic urine, which comprises fucoidan or a fucoidan-containing material as an active ingredient and can increase the pH vale of the urine in a sustained manner. Also disclosed is use of fucoidan or a fucoidan-containing material for the production of the food/beverage or pharmaceutical composition. Further disclosed is a method for improving an acidic urine by increasing the pH value of the urine in a sustained manner, which is characterized by orally administering fucoidan or a fucoidan-containing material.
CA2230350C Combination preparation for use in dementia A combination preparation comprising a compound which has an acetylcholinesterase-inhibitory action or exhibits muscarinergic action and a compound which increases the endogenous extracellular adenosine level is suitable for the treatment of dementia.
WO2008096046A1 Noroxymorphone for use as a medicament The present invention concerns noroxymorphone and its use in the manufacture of an intrathecally or systemically applicable medicament for the treatment of pain and inflammation. The invention also concerns a composition comprising noroxymorphone. The present invention also relates to a novel method for producing a medicament comprising noroxymorphone. The invention also relates to a method of treating pain in a subject by administering the subject with an analgesically effective amount of noroxymorphone.
CN102670590A Application of benzamide compound The invention discloses application of a benzamide compound shown as a formula I in preparation of a nicotinamide phosphoribosyl transferase inhibitor and application of the compound I in preparation of a medicament for preventing and/or treating cancers. The brand-new application of the compound I is discovered, namely the compound has good inhibiting activity for nicotinamide phosphoribosyl transferase, can be used for preparing the medicament for preventing and/or treating diseases by inhibiting the nicotinamide phosphoribosyl transferase, and can also be used for preventing diseases such as cancers.
CN103230014A Composition capable of increasing bone mineral density The invention relates to a composite capable of increasing bone mineral density. The composition is characterized in that active components for preparing the composition comprise 5-25g of calcium carbonate, 4-20g of glucosamine hydrochloride and the like by weight.
CN101390835B Ribavirin soluble powder The invention relates ribavirin soluble powder and the preparation method thereof. Ribavirin, and fosfomycin sodium are used as main ingredients, together with proper amount of perfume, soluble flavoring agent and soluble filler; the ribavirin soluble powder is prepared through the following conventional methods, drying, weighing, crushing, stirring, homogenized mixing, inspection, measuring and packing. The ribavirin soluble powder has the advantages of simple application, low cost, complete aroma, stable storage, convenient transportation and good water solubility; the ribavirin soluble powder can be prepared into drinking agent to improve the treatment effect of ribavirin for the non-food animals so that the ribavirin soluble powder is special non-food animal powder which is novel, broad-spectrum and efficient.
CN102241608A Retigabine compound and composition thereof The invention relates to a retigabine compound in a semihydrate crystal form and a preparation method thereof. The compound in the crystal form has the following good characteristics: the purity is high; and the stability is good, and the compound has superiority in industrial production and is suitable for preparation technological process and long-term storage. The invention also relates to a pharmaceutical composition of the retigabine compound in the semihydrate crystal form and an application of the compound in preparation of antiepileptic medicaments.
US20110171305 Dehydrated hydrogel inclusion complex of a bioactive agent with flowable drug delivery system The invention provides a controlled release biodegradable polymer formulation adapted for administering bioactive agents such as therapeutic proteins to a patient through implantation of a bolus that forms a depot within the patient's body tissues. The formulation includes a dehydrated inclusion complex of the bioactive agent within a hydrogel, wherein the hydrogel can comprise a polymerized polyalkyleneglycolyl diacrylate, and, optionally, polyalkyleneglycolyl monoacrylates, including methacrylates. Alternatively, the hydrogel can comprise hyaluronic acid, chitosan, agarose, polyvinylacetate, polyvinylpyrrolide, or polyvinylalcohol nanoparticles. The bioactive agent can be a macromolecular material, such as a protein. A method of forming the inventive formulation is also provided, as well as a method for using the formulation in the treatment of a malcondition in a patient in need thereof.
US20100196507 Treatment of Wounds and Compositions Employed A synthesized composition containing zinc ions, calcium ions, rubidium ions and/or potassium ions in a pharmaceutically acceptable carrier, which, when applied to an open wound, effectively modulates the activity of at least MMP-2 and/or MMP-9 in the wound. A method for treatment of wounds is disclosed.
CN101502514A Rifaximin enteric sustained-release preparation composition and method for preparing the same The invention discloses a rifaximin enteric sustained-release preparation combination and a preparation method thereof. The rifaximin enteric sustained-release preparation combination is mainly prepared from rifaximin bulk drugs, medicinal sustained-release and enteric materials and other appropriate auxiliary materials. The rifaximin enteric sustained-release preparation provided by the invention can not only prevent rifaximin from disintegrating in the stomach and causing irritation to gastric mucosa and avoid the adverse reactions caused by the administration, such as nausea, abdominal pain, diarrhea and the like, but also deaccelerate the release rate of drugs, reduce the frequency of administration and improve the patient compliance. The invention provides a novel form of drug having higher safety and better patient compliance and having the advantages of high quality controllability and stability of the preparation process.
CN103142615A Ceftriaxone sodium pharmaceutical composition and preparation method thereof The invention provides a ceftriaxone sodium pharmaceutical composition and a preparation method thereof, relating to the field of a medicinal preparation and a preparation method thereof. The invention mainly solves the problems of high dosage of single ceftriaxone sodium and metronidazole preparation, poor treatment effect after combination, and great side effect in the prior art. The pharmaceutical composition comprises ceftriaxone sodium and metronidazole lipid microspheres in a weight ratio of 100:3-100:10, wherein the weight of the metronidazole lipid microspheres is metered on the basis of metronidazole; and when the pharmaceutical composition is prepared into a powder injection, the pH value of the water solution of the pharmaceutical composition is 6.5-7.0. The pharmaceutical composition powder injection provided by the invention has high curative effect, and can reduce the consumption of the metronidazole by more than 80%, thereby greatly relieving or avoiding the toxic and side effects of the metronidazole, especially digestive tract reactions, including nausea, vomit, inappetence, abdominal colic and neurotoxicity, and lowering the incidence rate of adverse reactions.
US7314876 Administering to mammals nitrogen compounds, as mitogen activated kinase inhibitors, for prophylaxis asthma, respiratory system disorders, graft versus host disease, atherosclerosis and arthritis Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are surprisingly advantageous as p38 kinase inhibitors, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, NH2, or NH(CH3), preferably methyl; X is N or CH; and R1 through R6 are as described in the specification.
CN103222987A Food mineral supplement capable of effectively treating lupus erythematosus The invention discloses a food mineral supplement capable of effectively treating lupus erythematosus and relates to the fields of foods and medicines. The physiological action is that the low blood calcium condition of the human body can be directly corrected by moderately supplementing the minerals by virtue of three meals a day. The pH value in body fluid is lowered (pH lower than 7.35) due to the long-term low blood calcium, so that Ca<2+> external flow, Na<+>Cl<-> external flow and K<+> internal flow in lymphocyte B in the human body are caused, and therefore, juvenile cells are generated and excessively proliferated to generate excessive antibodies (i.e., specific immunoglobulin), and the excessive antibodies act on the texture cells of the human body to form autoimmune disease. The immune compound, which is difficult to degrade and polymerized into a macromolecule, is infiltrated and deposited in the human tissue, so that micro vessels are blocked to form systemic vasculitis which is the pathological basis of lupus erythematosus and the primary cause of various diseases. Therefore, the food mineral can be supplemented for effectively preventing and treating the lupus erythematosus. The conclusion has been testified in a plurality of clinical practices.
WO2011009095A1 Crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quin0lin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide This invention relates to three crystalline forms of N-[3-fluoro-4-((6-(methyloxy)- 7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl |oxy)phenyl]-N'-(4- fluorophenyl)cyclopropane-l.l-dicarboxamidc. Compound (I), designated as Form A, Form B, and Form C. The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline form of Compound (I) and a pharmaceutically acceptable excipient.
CN101928243B Acenaphtho heterocyclic compounds, and cyclodextrin inclusion compounds or conjugates thereof and application thereof in preparing Bcl-2 family protein inhibitors The invention relates to acenaphtho heterocyclic compounds, and cyclodextrin inclusion compounds or conjugates thereof and application thereof in preparing Bcl-2 family protein inhibitors. The acenaphtho heterocyclic compounds are obtained by introducing various oxo-substances, thio-substances, carbonyl compounds, ester compounds and acyl compounds to the 3, 4 and 6 sites in 8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-nitrile or further substituting acids, esters or amides for 9-nitrile. The compounds stimulate BH3-only proteins and competitively bind and antagonize Bcl-2, Bcl-xL and Mcl-1 proteins in vitro and in the cells, thus inducing cell apoptosis. The cyclodextrin inclusion compounds or conjugates can improve the effects of the compounds. The compounds and the cyclodextrin inclusion compounds or conjugates thereof can be used for preparing anti-cancer compounds.
WO2013081118A1 Compound having read-through activity (Problem) To provide a novel compound having read-through activity, and a therapeutic agent for nonsense mutation diseases containing the compound. (Solution) A compound represented by the general formula (1), and a pharmaceutical composition containing the compound.
US20060229299 5ht2c Receptor antagonists in the treatment of schizophrenia The present invention relates to the use of certain 5-HT2C receptor antagonists in the manufacture of medicaments for the treatment of mental disorders, in particular aspects of schizophrenia, cognitive impairment and suicidality, as well as to methods for determining the suitability of compounds for such a use.
WO2013171164A1 Compositions and formulations for the treatment of halitosis An orally disintegratingcomposition comprising a chelate comprising a metal ion and abiologically acceptable amino acid and having the general formula wherein M is the metal ion Zn2+ and R is H in the biologically acceptable amino acid glycine, use of the composition for the treatment of halitosis, and a chewing gum for the treatment of halitosis comprising a chelate comprising a metal ion and a biologically acceptable amino acid and having said general formula, which chewing gum is based on a carrier composition comprising a gum base, sorbitol, xylitol, one or more plasticizer(s), and one or more anticaking agent(s).
EP2677884A1 Ketogenic diet composition for the treatment of chemo therapy and/or radiation therapy patients The present invention provides ketogenic compositions for use in the treatment of a cancer patient undergoing chemotherapy or radiation therapy.
WO2007058568A3 Salts of 9-oxoacridine-10-acetic acid with 1-alkylamino-1-desoxy-polyols The invention relates to 1-alkylamino-1-desoxy-polyols and 9-oxoacridine-10-acetic acid salts of general formula (I), wherein A is (II), in which R is selected from an ethyl, propyl and butyl group, to medicinal preparations containing an active agent embodied in the form of one or several salts of formula (1) according to item 1 and/or the mixture of said salt of formula (I) or the 9-oxoacridine-10-acetic acid of formula (III) with one or several 1-alkylamino-1-desoxy-polyols of general formula (II), wherein R is selected from the ethyl, propyl and butyl group.
US20100222319 Nicotinamide derivatives, preparation thereof and therapeutic use thereof The disclosure relates to compounds of formula (I): wherein A, Z, Z′, L, R2 and R3 are as defined in the disclosure, to compositions comprising said compounds, and to methods for the manufacture and therapeutic use thereof.
WO2007130780A3 Benzimidazole modulators of vr1 The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.
CA2738605A1 Composition and method for treatment of preterm labor The invention provides a method for treating or preventing preterm labor in pregnant female subjects. The method comprises the step of administering a therapeutically effective amount of a Toll-like Receptor 9 antagonist sufficient to prevent the activation of Toll-like Receptor 9 by fetal DNA. The invention further provides compositions comprising a Toll-like Receptor 9 antagonist for use in the methods of the invention. Said compositions and methods enhance gestation and therefore improve neonatal morbidity and mortality.
EP1071422B1 Association of Riluzole and levodopa for the treatment of Parkinson disease The invention concerns a combination of levodopa and riluzole or a pharmaceutically acceptable salt of said compound and the use of said combination for treating Parkinson disease.
US20080027012 Bridged carbamate macrolides The present invention discloses compounds of formulae (I) and (II) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
CA2174106C Imidazo[1,5-a]quinolines for treatment of anxiety and sleep disorders The present invention is to imidazo[1,5-a]quinolines (I) which are useful pharmaceutical agents for the treatment of anxiety, sleep disorders, panic states, convulsions and muscle disorders. Compounds according to the invention have the general chemical structure of formula (I):(see formula I)
US20110033448 Inhibitors of LL-37 Mediated Immune Reactivity to Self Nucleic Acids Methods and compositions for treating disease are provided. More particularly, methods and compositions of inhibiting pathogenic interferon production are prevented, which may be useful in the treatment of various diseases. In other embodiments, therapeutic compounds and methods for the treatment of autoimmune diseases and chronic inflammatory diseases are provided. One such method is a method for inhibiting pathogenic interferon production or inhibiting activation of plasmacytoid dendritic cells or treating an autoimmune or chronic inflammatory disease, which comprises inhibiting one or more of LL-37 and hCAP18.
CN103204782A Levocarnitine compound The invention belongs to the technical field of medicines and in particular relates to a chloracetyl-levocarnitine compound. The chloracetyl-levocarnitine is also called as acetyl levocarnitine hydrochloride and is hydrochloride of acetyl-levocarnitine. The acetyl levocarnitine (ALC) is trimethyl amino-acid ester and is synthesized by acetyl levocarnitine transferase in the brain, liver and kidney in vivo. The levocarnitine compound can be used for promoting ingestion of acetyl coenzyme A by mitochondria in a fatty acid oxidation process, increasing the generation of acetyl choline and stimulating the generation of protein and lecithin. The invention further provides an application of the chloracetyl-levocarnitine compound to medicines for treating diabetic neuropathy.
US20080311193 Sustained Release Formulation of Alprazolam The present invention is directed towards the preparation of extended release Alprazolam formulation. The formulation thus obtained provides an efficient mode of delivery of Alprazolam in a continuous manner.
WO2009158526A2 Methods of reducing cellular proliferation by inhibiting acsvl3 The present invention is directed to methods of reducing cancer cell proliferation and/or treating cancer by administering a therapeutically effective amount of a compound that inhibits the activity of ACSVL3.
CA2355493C Therapeutic compositions comprising excess enantiomer The present invention is concerned with pharmaceutical compositions comprising a mixture of amlodipine enantiomers, which compositions have both anti-hypertensive and additional cardiovascular properties derived respectively from their calcium channel-blocking activity and their ability to release vascular nitric oxide (NO).
EP1486500B1 10-(3-cyclopropylaminomethyl-1-pyrrolidinyl)pyridobenzoxazinecarboxylic acid derivative effective against resistant bacteria A compound represented by the general formula (I): (I) wherein R1 represents methyl, fluoromethyl, methoxymethyl, acetoxymethyl, hydroxymethyl, or methylene; R2 represents hydrogen, C1-3 alkyl, or a pharmaceutically acceptable ester group of a cation and a prodrug; R3 represents hydrogen or halogeno; R4 represents hydrogen, C1-3 alkyl, fluoromethyl, trifluoromethyl, or fluorine; and R5 represents hydrogen or fluorine. It has excellent antibacterial activity against gram-positive bacteria, in particular, resistant bacteria such as MRSA, PRSP, and VRE.
CN101804089B Use of total flavonoids from radix Daphne genkwa in preparing weight-losing hypolipemic drugs The invention relates to a use of total flavonoids from radix Daphne genkwa plants in preparing weight-losing hypolipemic drugs, especially weight losing, which achieves the purpose of losing weight and simultaneously can lower the content of TC, TG and LDL-C and raise the content of HDL-C.
US20110097333 Therapeutic and diagnostic agents The present invention relates generally to therapeutic and diagnostic agents. More particularly, the present invention provides molecules having structural features characteristic of immunoregulatory signalling (IRS) molecules and which are expressed by cells of haematopoietic lineages such as, in particular, leukocytes. The molecules of the present invention find broad application inter alia as diagnostic markers for cells, targets for cell therapy and as validated drug targets in order to modulate the immune response and to treat, prevent and diagnose a range of diseases conditions including cancer, genetic disease, inflammatory conditions and conditions associated with aberrant haematopoietic cell function or activity. The present invention extends to binding partners of the instant molecules such as, for example, antibodies, ligands, adaptor and other signalling associated molecules, agonists and antagonists and to methods of screening for same.
US20100130401 Protein hydrolysate and plant sterol containing composition for improving serum lipid profile and preventing atheroscleroris The invention relates to a terapeutical composition comprising a protein hydrolysate and a plant sterol, wherein the weight ratio of the plant sterol to the protein hydrolysate is from 1:0.02 to 1:150. The invention also relates to a terapeutical composition comprising a protein hydrolysate and a synthetic emulsifier and/or a lipid based grain fraction having emulsifying properties. Said compositions can be used in a pharmaceutical, nutraceutical or food product for improving serum lipid profile.
US20120172408 Active ingredient comprising indocyanine green and/or infracyanine green The present invention relates to an active ingredient including indocyanine green and/or infracyanine green for use in treating dental or periodontal infectious diseases under irradiation with light, more particularly laser light, from a wavelength range between 790 nm and 830 nm.
CN102772413A Low dose entecavir formulation and use Compositions containing a low dose of entecavir are administered on a daily basis to treat hepatitis B virus infection and/or co-infections. Formulations for the oral administration of a low dose of entecavir are provided. Other pharmaceutically active substances can be included in the entecavir composition or can be separately administered for the treatment of hepatitis B virus infection or for the treatment of co-infected patients.
CN1899430A Large size Qingkailing dripping pill and its preparing method The present invention discloses a kind of large size Qingkailing dripping pill over 100 mg each and its preparation process. The large size Qingkailing dripping pill has convenient taking, high bioavailability, quickly release of effective components, quick acting and less toxic side effect.
WO2005123772A3 Anti-cancer therapy A method of prevention progression from chronic inflammatory condition to cancer, by administration an NF- B inhibitor, anti TNF agent or an NSAID. The method can also be used to prevent cancer in an individual having a high probability (genetic) of developing the types of cancer usually associated with inflammation.
CN101099724A Micronization femara and its composition The present invention discloses a kind of micronized letrozole and its composite. Said invention utilizes a micronization process to micronize said letrozole and make the micronized letrozole be combined with a proper carrier so as to obtain a micronized letrozol preparation with proper dissolubility. Said preparation can be used for effectively curing mammary cancer.
WO2008019825A1 Use of tricyclic indole derivatives for the treatment of muscular diseases The present invention relates to the use of a compound for the preparation of a medicament for the treatment of muscular atrophy.
WO2013154209A1 Antiprotozoan composition containing caspofungin or its salt and biguanide compound or its salt The present invention relates to an antiprotozoan composition containing caspofungin or its salt and a biguanide compound or its salt.
CN101596203B Application of syringin in preparing drugs for treating cardiovascular and cerebrovascular diseases The invention relates to application of syringin in preparing drug combination for treating cardiovascular and cerebrovascular diseases. The syringin preparation is safe and nontoxic and has strong pharmacological action and good drug effect, thereby indicating bright prospect in drugs; the syringin preparation is simple in preparing process, has no toxic side effects and can be in oral forms such as tablets, pills, capsules and the like, or in injectable forms such as powder-injection, instillations and the like; the drugs prepared by the syringin can evidently lessen the degree and scope ofmyocardial ischemia caused by the anterior descending branch of canine coronary artery, reduce the myocardial oxygen consumption index, obviously withstand barium chloride induced arrhythmia in rats and reduce the cerebral infarct area of focal cerebral ischemia in rats; the above effects show that the drugs have obvious effects against arrhythmia, myocardial ischemia and cerebral ischemia. The drugs can be clinically used for preventing and treating coronary diseases, angina, stroke and cerebral infarct, etc.
WO2007086799A1 Amide substituted quinolines Compounds of Formula I [Chemical formula should be inserted here. Please see paper copy] wherein R1, A, R2, n, R3, m, R4, R5 and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
EP1584619A1 Derivatives of quinoline as inhibitors for MEK 1. A compound of formula (I) or a pharmaceutically acceptable salt thereof. wherein: n is 0-1; X and Y are independently selected from -NH-, -O-, -S-, or -NR8- where R8 is alkyl of 1-6 carbon atoms and X may additionally comprise a CH2 group; R7 is a group (CH2)mR9 where m is 0,or an integer of from 1-3 and R9 is a substituted aryl group, an optionally substituted cycloalkyl ring of up to 10 carbon atoms, or an optionally substituted heterocyclic ring or an N-oxide of any nitrogen containing ring; R6 is a divalent cycloalkyl of 3 to 7 carbon atoms, which may be optionally further substituted with one or more alkyl of 1 to 6 carbon atom groups; or is a divalent pyridinyl, pyimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally further substituted with one or more specified groups; R1, R2, R3 and R4 are each independently selected from hydrogen or various specified organic groups. Compounds are useful as pharmaceuticals for the inhibition of MEK activity.
US20100015208 Antibacterial wound dressing The present invention relates to wound dressings, in particular to an antibacterial wound dressing based on silvered gel-forming fabric and to a process for the manufacture of such a wound dressing.
EP2039695A1 Bicyclic heterocyclic compound and use thereof The present invention provides a bicyclic heterocyclic compound having a serotonin 5-HT2c receptor activation action and the like. A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
EP2720720A1 Combination therapy to prevent dcis formation and progression to breast cancer A method of treating a ductal carcinoma in situ (DCIS) lesion in a subject in need thereof is disclosed. The method comprises administering to the subject a therapeutically effective amount of a first agent capable of down-regulating activity and/or expression of at least one component participating in a NOTCH pathway, and a second agent capable of down-regulating an activity and/or expression of HER2, thereby treating the DCIS lesion.
US20100172990 Biocompatible microgels and applications thereof The biocompatible microgels comprises a polymeric network, said polymeric network comprising monomeric units interconnected with one another through a crosslinking agent, wherein said polymeric network can be obtained by polymerization in a dispersed medium of a biocompatible vinyl monomer and a crosslinking agent. The microgel may further comprise a biologically active agent. Said biocompatible microgels can be used, among other applications, to transport and dose biologically active agents.
DE102005047561A1 Drug delivery system, useful to treat and/or prevent e.g. thromboembolic disease, comprises 5-chloro-N-(((5S)-2-oxo-3-(4-(3-oxo -4-morpholinyl)-phenyl)-1,3-oxazolidine-5-yl)-methyl)-2-thiophene carboxamide with fast release active substance Solid, orally administrable pharmaceutical drug delivery system (A) comprises 5-chloro-N ({(5S)- 2-oxo-3-[4-(3-oxo-4-morpholinyl)- phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamide (I) with a fast release of the active substance, where the active substance (I) is in amorphous form and 80% of the active substance (I) is released within less than 2 hours, according to United State Pharmacopeial drug release procedure with apparatus 2 (Paddle). Independent claims are included for: (1) a method for the preparation of (A) comprising preparing the active substance (I) containing a mixture by a melt process, mixing the obtained mixture in powder form with further auxiliary materials and subsequently filling the mixture as sachet or capsules, or after mixing with tableting additives, preferably by direct tableting and press-molding to tablets, which is subsequently polished; (2) a mutli-particulate pharmaceutical drug delivery system; (3) a pharmaceutical drug delivery system comprising the multi-particulate pharmaceutical drug delivery system; (4) a method for the preparation of multi-particulate pharmaceutical drug delivery system comprising preparing active substance (I) with an extrudate by melt extrusion process and cutting the obtained mixture; and (5) a method for prophylaxis, secondary prophylaxis and/or treatment of thromboembolic diseases comprising administering (A). - ACTIVITY : Thrombolytic; Cardiant; Antianginal; Vasotropic; Cerebroprotective; Anticoagulant. - MECHANISM OF ACTION : Factor Xa inhibitor.
CN101152188A Vitamin D* solid dispersion peridium patch and method for preparing the same The invention relates to Vitamin D2 solid dispersion coated tablet and the preparation method, belonging to pharmaceutical preparation technical field. The tablet contains Vitamin D2 and pharmaceutical excipient, with Vitamin D2 as the active component. Every ten thousand tablets contain 0.3125g of Vitamin D2, 100g of PEG-6000, 2500g of starch, 2250g of phosphoric acid calcium hydrogen, 75ml of alcohol, 100g of magnesium stearate and 50g of talc. The invention has a simple preparation method, according to which Vitamin D2 is coated to produce tablets. The Vitamin D2 tablets prepared in the method has obvious treating effects and can be taken orally. The toxicity is low and the bioavailability is greatly enhanced. Besides, the tablet has the functions of sustaining, targeting, energy provision for human organism, etc.
CN103113349A 4-imidazolyl quinoline and quinazoline ketone aromatizing enzyme inhibitors as well as preparation method and medical application thereof The invention relates to the field of medicinal chemistry and in particular relates to 4-imidazolyl quinoline and quinazoline ketone aromatizing enzyme inhibitors. The invention further discloses a preparation method and pharmacological activity of the inhibitors, a medicinal composition containing the compounds as well as the medical application of the inhibitors, in particular the medical application of the inhibitors in preventing or treating estrogen maintaining diseases such as breast cancers, endometrial cancers, female sexual precocity, gynecomastia and the like.
US20120070480 Antimicrobial disposable absorbent articles Disposable absorbent articles comprising an absorbent material and an antimicrobial composition are disclosed. The antimicrobial composition includes a carrier comprising fatty alcohol and a poly(alkyleneoxy) polymer, and an antimicrobial agent. The antimicrobial composition may be coated on to component substrates such as nonwovens and films, that are incorporated into disposable absorbent articles, such as disposable infant diapers, adult incontinence articles, feminine hygiene articles such as sanitary napkins, wound dressings, bandages, panty liners and tampons, personal care wipes and household wipes to provide odor control, and control of microbial growth.
WO2007101531A1 Use of adenosine a1 and/or dual a1/a2b agonists for production of medicaments for treating diseases The invention relates to use of A1 and/or dual A1/A2b agonists of formula (IA) and (IB) for production of a medicament for treatment of dyslipidemia, metabolic syndrome and diabetes and dyslipidemia, metabolic syndrome and diabetes in connection with hypertonia and diseases of the cardiovascular system.
EP1582212A1 Intravitreally-injectable solution for the treatment of vitreous haemorrhages The present invention relates to an ophthalmic solution for the clarification of vitreous hemorrhages. More specifically, it relates to a pharmaceutically acceptable intraocular injectable solution, for the treatment of vitreous hemorrhages, whereby the reabsorption of such hemorrhage is encouraged. It enables the clarification of the vitreous hemorrhage in a significantly short period of time to allow for the timely diagnosis of the lesion and the repair of the damage the hemorrhage has caused to the vitreous body. The ophthalmic solution of the present invention is injected at least once into the vitreous humor of the patient in a therapeutically effective dose to obtain the desired result.
WO2009034062A1 Compounds which inhibit the glycine transporter and uses thereof in medicine Compounds of Formula (I) and salts thereof are provided: wherein the groups are as defined in the specification. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
US20100222408 Methods and Compositions for Treatment of Cystic Fibrosis The present invention relates to compounds and methods of inhibiting p97/valosin-containing protein and compounds and methods of inhibiting gp78, the compounds and methods being useful for the treatment of a disorder comprising a IκB/NFκB mediated chronic inflammatory response component, for example cystic fibrosis.
WO2007093226A1 Oral ibandronate formulations The present invention provides novel solid pharmaceutical dosage forms for oral administration comprising a bisphosphonate, or a pharmaceutically acceptable salt thereof, which bisphosphonate is present in an amount not therapeutically effective when the bisphosphonate is orally administered alone; and a modified amino acid carrier, or a pharmaceutically acceptable salt thereof, which modified amino acid carrier is present in an amount effective to facilitate absorption of the bisphosphonate in the gastrointestinal tract such that the bisphosphonate is therapeutically effective. The ratio of bisphosphonate to modified amino acid carrier is from about 1:30 to about 1:1, respectively. These novel solid pharmaceutical dosage forms are useful in the treatment or control of bone diseases and particular disorders in calcium metabolism, including, for example, osteoporosis, hypercalcemia of cancer, and the treatment of metastatic bone pain. The present invention also provides a method for treating these diseases employing the solid pharmaceutical dosage forms and a method for preparing the pharmaceutical dosage forms.
WO2013174931A1 7-oxo-4,7 -dihydro- pyrazolo [1, 5 -a] pyrimidine derivatives which are useful in the treatment, amelioration or prevention of a viral disease The present invention relates to a compound having the general formula (C), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
US20100041744 Oily paclitaxel composition and formulation for chemoembolization and preparation method thereof Oily paclitaxel composition and formulation for chemoembolization and preparation method thereof solubilizing paclitaxel in an oily contrast medium. The composition of the present invention solubilizes paclitaxel and has an advantage of delivering anticancer drug to the target cells by chemoembolization since it is possible to visualize the blood vessel during the chemoembolization process. The present invention also relates to oily paclitaxel composition and formulation additionally comprising chemicals that prevent paclitaxel precipitation for prolonged preservation and the preparation method thereof. Since the composition of the present invention solubilize paclitaxel effectively and can be visualized during chemoembolization, it can be used for TACE to treat hepatoma and other solid tumors.
CA2438169C Modulated release particles for aerosol delivery A modulated release aerosol formulation is disclosed. The formulation comprises a polymer, e.g. Silica gel, fumed silica gel, having a selected medicament associated therewith, and a fluid carrier for carrying and delivering the construct.
CN102711770A Cerebral nerve cell neogenesis agent Disclosed are: a novel substance having a cerebral nerve cell neogenesis effect; and a cerebral nerve cell neogenesis agent which comprises the substance and is effective for the treatment and/or prevention of nerve diseases. Specifically disclosed is a cerebral nerve cell neogenesis agent comprising a plasmalogen as an active ingredient. Particularly, a cerebral nerve cell neogenesis agent comprising, as an active ingredient, a plasmalogen extracted from a biological tissue (preferably an avian tissue) that mainly contains ethanolamine plasmalogen and choline plasmalogen is preferred.
CN1857725A Slow released compound antituberculotic preparation containing synergist The slow released compound antituberculotic preparation containing synergist is implanting agent or slow released injection comprising slow released microsphere and solvent. The slow released microsphere consists of slow releasing supplementary material, at least one antituberculotic selected from rifampicin, isoniazid and pyrazinamide and at least one antituberculotic synergist selected from cycloserine, ofloxacin, ciprofloxacin, sparfloxacin and capreomycin. The solvent is special solvent containing suspending agent carboxymethyl cellulose, etc. and with viscosity of 100-3000 cp at 20-30 deg.c. The slow releasing supplementary material is selected from EVAc, PLA, PLGA, etc. The slow released compound antituberculotic preparation can release antituberculotic in the local tubercolosis part for 30-40 days so as to maintain the local effective medicine concentration while lowering systemic toxicity. The present invention has obvious unique treating effect on various kinds of intractable tuberulosis.
WO2013169741A1 Agents and devices for affecting nerve function Agents and devices for affecting nerve function are described. In some variations, a combination of agents, e.g., a cardiac glycoside, an ACE inhibitor, and an NSAID are delivered to affect nerve function. The agent may be delivered locally in a site-specific manner to a targeted nerve or portion of a nerve. For example, the agent may be delivered locally to the renal nerves to impair their function and treat hypertension. One variation of a delivery device includes one or more needle housings supported by a balloon. A delivery needle is slidably disposed within a needle lumen of each needle housing.
CN101845034A Preparation and application method of scutellarin The invention discloses a preparation method of scutellarin, comprising the following steps of: (1) refluxing and extracting a medicinal material of erigeron breviscapus with ethanol; (2) filtering a leaching solution in the last step and carrying out pressure reduction to recover ethanol to obtain extract for later use; (3) respectively extracting with petroleum ether, ethyl acetate and normal butanol to obtain a petroleum ether extraction part, an ethyl acetate extraction part and a normal butanol extraction part; (4) dissolving the ethyl acetate part with ethanol; (5) adding silica gel and stirring, naturally drying, porphyrizing and sieving to obtain fine powder; (6) through gel column chromatography, carrying out gradient elution on the petroleum ether and the ethyl acetate and collecting by section; and (7) carrying out gel column chromatography on the ethyl acetate extraction part and elution by the petroleum ether and isopropanol and checking and combining same speckle parts according to a thin layer to obtain a compound of scutellarin. The scutellarin extract is used as an active component and is used for preparing a medicine for preventing and treating neurodegenerative diseases. The method can be used for preparing the scutellarin the purity of which is as high as 95 percent; and the raw material can be used for preparing a medicine for treating senile dementia and serves the human health.
WO2006063025A1 Stable non-crystalline formulation comprising donepezil One or more embodiment of the invention provide various novel formulations comprising donepezil that are non-crystalline, more stable, and/or otherwise improvements over known donepezil formulations. The donepezil-containing formulations may be administered to a user to treat senile dementila, especially the Alzheimer type.
US20080039522 Composition Containing a Complex Comprising a Metal Ion and a Carboxylate Ligand Having Anti-Inflammatory Activity A pharmaceutical composition comprising a metal complex of a carboxylate having anti-inflammatory activity in a pharmaceutically acceptable carrier, wherein: (1) the composition has a colloidal structure, or forms a colloidal structure when administered to a human or animal, or is immiscible with water; (2) more than 80% of the total amount of the carboxylate having anti-inflammatory activity in the composition is present as part of a metal complex; and (3) less than 10% of the carboxylate having anti-inflammatory activity complexed with the metal dissociates from the metal over 12 months when the composition is stored in the absence of light at room temperature; but excluding compositions comprising a metal complex containing the ligand DMF. The invention also provides the use of the pharmaceutical composition in the treatment of inflammatory conditions in humans and animals.
CN103110566A External pigmentum for correcting bad habit of finger sucking of infants The invention discloses an external pigmentum for correcting a bad habit of finger sucking of infants. The external pigmentum consists of bitters and a water-insoluble film-forming agent and is applicable to correcting a finger sucking habit, a pencil biting habit and the like of infants. If necessary, the external pigmentum can be also applied on nipples of a foster-nurse when the infants are weaned off breast feeding.
WO2006006172A3 Use of anti-amyloid agents for treating and typing pathogen infections A method of preventing or treating a pathogen infection in a subject is provided. The method comprising administering to a subject in need thereof a therapeutically effective amount of an anti amyloid agent, thereby treating or preventing the pathogen infection in the subject.
CN102988350A Application of Aphanamixoid A in influenza A virus (Flu-A) resistant medicine The invention discloses application of Aphanamixoid A in an influenza A virus (Flu-A) resistant medicine. Experiments prove that Aphanamixoid A has obvious inhibitory effect on Flu-A, which prompts that Aphanamixoid A has potential application value in the field of treating Flu-A infectious diseases. The application of Aphanamixoid A for preparing the medicine for treating influenza virus infection is disclosed for the first time; because the skeleton type belongs to a brand new skeleton type and the Flu-A inhibitory activity of Aphanamixoid A is strong unexpectedly, the possibility that other compounds give any inspiration does not exist; Aphanamixoid A has outstanding substantive characteristics; and simultaneously, Aphanamixoid A has obvious progress for preventing and treating influenza virus infection.
CN101022809A Dihydropteridinones for the treatment of cancer diseases The present invention relates to the use of a compound of general Formula (1), optionally in form of its tautomers, racemates, enantiomers, diastereomers and the mixtures thereof and optionally in form of the pharmacologically acceptable acid addition salts, solvates, hydrates, polymorphs, physiologically functional derivatives or prodrugs thereof, for the preparation of a pharmaceutical composition for the treatment of diseases characterized by abnormal cell proliferation in a human or non-human mammalian body by inhibition of polo like kinases as mitotic regulators.The present invention relates to the use of a compound of general Formula (1), for the treatment of diseases characterized by abnormal cell proliferation in a human or non-human mammalian body by inhibition of polo like kinases as mitotic regulators like cancer selected from the group consisting of carcinomas, sarcomas, melanomas, myeloma, hematologic neoplasias, lymphomas, childhood cancers and leukemia, autoimmune disorders selected from the group consisting of amyloidosis, systemic lupus erythematosus, rheumatoid arthritis, Crohn's disease, multiphe sclerosis, systemic sclerosis (scleroderma), mixed connective tissue disease, Sjgren's syndrome, ankylosing spondylitis, autoimmune vasculitis, Behcet's syndrome, psoriasis, autoimmune arthritis, sarcoidosis, diabetes mellitus and fungous diseases.
EP1836201A1 Pyrrolidine inhibitors of iap The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I), wherein A,Q,X1,X2,Y,R1,R2,R3,R4,R4’,R5,R6 and R6’ are described herein.
EP1168934B1 Hydrogel-forming system with hydrophobic and hydrophilic components A hydrogel forming system which comprises a hydrophobic macromer with unsaturated group terminated ends and a hydrophilic polymer which is a polysaccharide containing hydroxy groups which are reacted with unsaturated group introducing compound, is convertible by free radical polymerization to form a hydrogel containing a three dimensional crosslinked polymer network containing hydrophobic and hydrophilic components. Preferably, the hydrophobic polymer is prepared by reacting the hydroxyls of a diol obtained by converting hydroxy of terminal carboxylic acid group of poly(lactic acid) to aminoethanol group, with an unsaturated group introducing compound which is acryloyl chloride or isocyanate having an unsaturated group at one end of the molecule. Preferably, the hydrophilic polymer is dextran wherein one or more hydroxyls in a glucose unit of the dextran is (are) reacted with an unsaturated group introducing compound which is acryloyl chloride or isocyanate having an unsaturated group at one end of a molecule. Agent can be entrapped in the polymer network, e.g., drugs, water-soluble macromolecules or synthetic or natural polymers, for controlled release therefrom.
CA2392050C Pharmaceutical formulations containing zolmitriptan A pharmaceutical formulation of the 5HT1-agonist, zolmitriptan, for use in intranasal administration. The formulation is useful in treating migraine and related disorders.
US8618146 Epothilone compound formulations The present application relates to compositions for parenteral administration of epothilone compounds, such as ixabepilone.
CN103599120A Nifuratel-nysfungin soft capsule suppository and preparation method thereof The invention discloses a nifuratel-nysfungin soft capsule suppository. The nifuratel-nysfungin soft capsule suppository comprises 500mg of nifuratel, 200000IU of nysfungin, 8mg of promestriene, 25mg of carbomer, 700mg of glycerinum, 6mg of ethylparaben, 294mg of triethanolamine, 800mg of ethyl alcohol and 7.5g of water. The invention also discloses a preparation method of the nifuratel-nysfungin soft capsule suppository. The nifuratel-nysfungin soft capsule suppository can kill bacteria, mould and trichomonad, effectively protect lactobacillus and promote vaginal flora to restore balance, thus realizing the purpose of 'ecological treatment'; and the soft capsule suppository has both the dosage form characteristic of soft capsule (good stability of capsule core, capsule skin and drug) and local drug delivery characteristic of suppository.
CN102091048A Preparation method and quality control method of arbidol hydrochloride tablet The invention relates to a preparation method and a quality control method of an arbidol hydrochloride tablet. The arbidol hydrochloride tablet comprises the following major ingredients: arbidol hydrochloride, microcrystalline celluloses, milk sugar, starch, low-substituted hydroxypropyl celluloses, talcum powder, magnesium stearate and a right amount of adhesive starch slurry. The preparation method of the arbidol hydrochloride tablet comprises the following steps of: preprocessing; preparing granules; and tabletting. The quality control method of the arbidol hydrochloride tablet comprises the following steps of: measuring dissolution rate, related substances and content. For overcoming the defects of the traditional variety, the invention provides the preparation method of the arbidol hydrochloride tablet, which has the advantages of broad spectrum, high efficiency, stable quality, simple process, low cost, easy patient acceptance, and the quality control method of the arbidol hydrochloride tablet, which has the advantages of convenience, fastness, accurate quantification, good specificity and high applicability.
WO2008142463A2 Carbamoyl-cyclohexanes for treating acute mania The present invention relates to use of (thio)-carbamoyl-cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N- dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment of acute mania. Furthermore, the present invention relates to the treatment of acute mania through the administration of (thio)- carbamoyl cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin- 1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof.
CN103539784A Heterocyclic benzamide compounds, pharmaceutical compositions as well as application thereof The invention discloses heterocyclic benzamide compounds with structural characteristics of formula (1) or pharmaceutically acceptable salts or steric isomers or prodrug molecules thereof. The heterocyclic benzamide compounds as well as pharmaceutically acceptable salts thereof can effectively restrain growth of a plurality of tumor cells, can generate inhibiting effect to proteases such as BCR-ABL, c-Kit and PDGFR, can be used for preparing anti-tumor drugs and can be used for overcoming existing drug (Gleevec)-induced drug resistance.
WO2008126886A1 Indole or indoline derivative Novel indole or indoline derivatives having a histamine H3 receptor antagonism, represented by the formula: (1) (wherein the double bond containing an undulating line is a single bond or double bond; Q is any of the groups of the structural formulae: (A) (B) R is a C1-C6 alkyl, -C(O)R4, etc.; R1 is a C1-C6 alkyl, etc.; and each of R2 and R3 independently is a C1-C6 alkyl, C3-C8 cycloalkyl, etc.), or pharmaceutically acceptable salts thereof, and pharmaceutical preparations containing any thereof as an active ingredient. These are useful in the prevention or treatment of diseases, such as cognitive deficit, Alzheimer, attention-deficit hyperactivity disorder, schizophrenia, eating disorder, obesity, diabetes mellitus, hyperlipemia, sleep disorder, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis, etc.
EP1426051B1 Medicinal composition for prevention of or treatment for cerebrovascular disorder A medicinal composition comprising: (a) a compound represented by the following general formula (I): (I) (wherein R1 represents hydrogen or hydroxy) or an acid addition salt or hydrate of the compound; and (b) at least one member selected from the group of acceptable drugs consisting of a cerebral vasodilator, vasodilator agent, brain-protective agent, cerebral metabolism activator, anticoagulant agent, antithrombocytic agent, thrombolytic agent, alleviator for mental disorders, hypotensive drug, remedy for angina pectoris, diuretic agent, cardiac restorative, antiarrhythmic agent, hyperlipemia remedy, and immunosuppressant. It is useful as a preventive or remedy for cerebrovascular disorders and cardiopathy.
EP1567126A2 Concentrated liquid valdecoxib composition The present invention provides a pharmaceutical composition comprising a liquid carrier, valdecoxib and cyclodextrin derivative in an amount of at least about 5%, w/v, of the composition. The valdecoxib is in solubilized form and, at room temperature, the ratio of valdecoxib concentration to cyclodextrin concentration is greater than is achievable in a substantially similar solution but which comprises less than 5%, w/v, of said cyclodextrin derivative.
CN101073553A Cromolyn-sodium eyes gel The invention is concerned with the method of preparation for the 1000ml. instant disodium cromoglicate ophthalmic gelatin. It contents: disodium cromoglicate 5-40g, antiseptic 0.05-1g, osmoregulation 1.0-7.5g, gel substrate 30-150g, and the certain amount of acid-base buffer and injection usage to fulfill the requested weight of the medicine. The invention enriches the pharmaceutical dosage form of the disodium cromoglicate that prolongs the residence time of the medicine at the eye areas, and improves the curative effect with no negative stimulation.
WO2012073214A3 Heptose derivatives for use in the treatment of bacterial infections Compounds having the general formula (I) pharmaceutical compositions containing them for use in inhibiting bacterial heptose biosynthesis and thereby lowering or suppressing bacterial virulence.
US20080138382 Biocompatible intraocular implants include a steroid and a polymer; biodegradable; eye implantable drug delivery systems; few or no negative side effects Biocompatible intraocular implants include a steroid and a polymer associated with each other to facilitate release of the steroid into an eye for a period of time greater than about two months. The steroid may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the steroid may be associated with a polymeric coating having one or more openings effective to permit the steroid to be released into an external environment. The implants may be placed in an eye to treat one or more ocular conditions. The steroid is released from the implant for more than about two months, and may be release for more than several years.
CN101524346A Application of conjugated linoleic acid (CLA) in preparing drugs for treating Alzheimer disease The invention discloses an application of conjugated linoleic acid (CLA) in preparing drugs for treating the Alzheimer disease. The invention is proved that the CLA has the effects of suppressing the expression of Beta-secretase, adjusting APP hydrolysis pathway and nurturing nerve cell on the premise without having influence to APP expression. The conjugated linoleic acid is a natural product, has characteristics of no toxicity to the human body and low side effect, can be used for preparing drugs for treating the Alzheimer disease and has wide application prospect.
WO2007052134A1 (2s)-2-aminomethyl-5-ethyl heptanoic acid its pharmaceutical use The present invention relates to (2S)-2-aminomethyl-5-ethyl-heptanoic acid and the pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing, and the uses of (2S)-2-aminomethyl-5-ethyl-heptanoic acid.
CN1939311B Ginseng sapogenin aglycone derivative biological preparation and its usage An antineoplastic compound 25mdt, that is, 20(s)-25-methoxyl-dammarane-3 beta, 12 beta, 20-triol, is a protopanoxadiol derivative, its antineoplastic medicine and its antineoplastic application is suppressing the growth and reproduction of tumor cells, inducing the differentiation and wither of tumor cells, preventing the transfer of tumor cells, improving immunity, and treating cancers are disclosed.
EP2073837A2 Recombinant modified vaccinia ankara encoding a her-2 antigen for use in treating cancer The invention relates to compositions, kits, and methods for cancer therapy using recombinant MVA viruses encoding a tumor-associated antigen, such as HER-2, particularly in combination with taxanes. The taxanes can be administered prior to, at the same time as, or after the recombinant MVA virus.
WO2012018635A2 Arylsulfonamide derivatives, compositions, and methods of use The present invention provides acylsulfonamides including bumetanide derivatives and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these compounds and methods for their use. All of these analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl- co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, attention deficit hyperactivity disorder (ADHD), autism spectrum disorders (autism), bipolar disorder, cancer, the improvement of cognitive function, cognitive impairment, cognitive dysfunction, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma, Huntington's Disease, inflammatory pain, insomnia, ischemia, migraine, migraine with aura, migraine without aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, periodic limb movement disorder (PLMD), personality disorders, postherpetic neuralgia, psychosis, restless legs syndrome (RLS), schizophrenia, seizure disorders, spasticity, tinnitus, and withdrawal syndromes.
EP0906335B1 Ebv type b ctl epitopes The present invention provides cytotoxic Epstein-Barr virus T-cell epitopes. These epitopes are QVKWRMTTL, VFSDGRVAC, VPAPAGPIV, TYSAGIVQI, LLDFVRFMGV, QNGALAINTF, VSSDGRVAC, VSSEGRVAC, VSSDGRVPC, VSSDGLVAC, VSSDGQVAC, VSSDGRVVC, VPAPPVGPIV, VEITPYEPTG, VEITPYEPTW, VELTPYKPTW, RRIYDLIKL, RKIYDLIEL and PYLFWLAGI. The present invention further provides vaccines including one or more of these epitopes, optionally with additional epitopes.
US7132397 Bone morphogenetic protein antagonist based on the mature protein The purpose is to provide a mature protein having an antagonistic activity against bone morphogenetic proteins. The mature protein having an antagonistic activity against bone morphogenetic proteins is obtained by converting at least one residue among methionine residues or tryptophane residues existing in the amino acid sequence of mature human MP52 (SEQ ID No 1) to a hydrophilic residue by chemical modification, or replacing said residues with a hydrophilic amino acid residue or a polar amino acid residue. The chemical modification for said methionine residue is performed by an oxidization reaction or an alkylation reaction. The chemical modification for said tryptophane residue is performed by an allylsulphenylation reaction. Or a mature protein having an antagonistic activity against bone morphogenetic proteins is obtained by converting at least one residue of tryptophane residues existing in the amino acid sequences of mature human BMP-2 (SEQ ID No 2), mature human BMP-4 (SEQ ID No 3), and mature human BMP-7 (SEQ ID No 4) to a hydrophilic residue by chemical modification, or replacing said residues with a hydrophilic amino acid residue or a polar amino acid residue.
US8501164 Nicotine lozenge compositions The present invention relates to nicotine lozenge compositions comprising reduced levels of buffering agents from traditional nicotine lozenges and which provide optimal oral pH and prompt nicotine absorption in a smaller, more convenient dosage form.
CN101703652A Mastic rheumatism aerosol and preparation method thereof The invention relates to a mastic rheumatism aerosol and a preparation method thereof. The mastic rheumatism aerosol is an aerosol or a spraying agent prepared by taking the raw material medicines of artificial musk, mastic, myrrh, borneol and draconis sanguis as main materials, adding the auxiliary materials of cinnamon oil, peppermint oil, eugenol type basil oil, methyl salicylate, laurocapram, eucalyptus oil, liquid paraffin, essence, a propellant and the like, extracting and preparing; the product has the effects of dispelling rheumatism, promoting blood circulation, relieving pain, decreasing swelling and the like; and the experiments of a plurality of clinical research organizations show that the mastic rheumatism aerosol has obvious curative effect to rheumatalgia, the pain of bones and muscles, the ache of the waist and legs, sciatica and traumatic injuries.
US20120196909 Deferacirox dispersible tablets The invention pertains to dispersible tablets comprising as active ingredient 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid or pharmaceutically acceptable salt thereof in an amount of from 5 to 40% in weight by weight of the total tablet.
US20100168091 Imidazole Amines As Inhibitors Of Beta-secretase The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated 3-amyloid deposits or 3-amyloid levels in a patient.
US20070244097 Nicotinic AcetylcholineReceptor Ligands Acetylcholine receptor ligands of formula I wherein D, E and G are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
US20120034189 Means and methods for durable inhibition of pathogens The invention provides improved nucleic acids for anti-HIV therapy. The invention further provides selection methods which are capable of predicting already at an early stage of development whether promising anti-pathogenic candidate compounds will be suitable for therapeutic use in vivo.
EP0751709B2 Use of bcl-2 for the manufacture of medicaments for the therapeutic treatment and prevention of diseases The invention provides a method of treating a disease or pathological condition resulting in apoptotic cell death. The method includes increasing the activity of Bcl-2 in cells affected by the disease or pathological condition. Diseases or pathological conditions can include, for example, neurodegenerative diseases, cancer and viral infections. Also provided is a method of prolonging the in vivo survival of transplanted cells for the treatment of a disease or pathological condition. The method includes increasing the activity of Bcl-2 in a population of cells and transplanting the population of cells having increased Bcl-2 activity into a subject. Diseases or pathological conditions can include, for example, neurodegenerative diseases, cancer and viral infections. A method to enhance the sensitivity of malignant cells to therapy is provided that includes decreasing the activity of Bcl-2 in the malignant cells. Methods to identify compounds that alter apoptotic cell death and to enhance monoclonal antibody production are also provided by the invention disclosed herein.
US7851461 Combination dosage of a cyclooxygenase (COX) inhibitor, a vitamin D3 including analogues and metabolites thereof and/or calcium for prevention of epithelial cancer The present invention relates to a method for prevention of epithelial cancer such as lung, bladder, prostate or gynaecological cancer or the initiation and/or progression of epithelial cancer such as lung, bladder, prostate or gynaecological cancer in a human comprising administering to the human of a combination dosage of a cyclooxygenase (COX) inhibitor, a vitamin D3 including analogues and metabolites thereof and/or calcium. In a further aspect the invention relates to a method for reducing the effective dosage of ASA in a chemopreventive treatment of epithelial cancer in a human by co-administration with a non toxic dosage of a vitamin D3 including analogues and metabolites thereof and/or Ca in the form of a combination dosage. In another embodiment the invention relates to the use of a cyclooxygenase (COX) inhibitor, a vitamin D3 including analogues and metabolites thereof and/or calcium for the preparation of a medicament for the prevention of epithelial cancer such as lung, bladder, prostate or gynaecological cancer or the initiation and/or progression of epithelial cancer such as lung, bladder, prostate or gynaecological cancer.
CN103739616A Thiazolyl-containing rapamycin type derivative and application thereof The invention relates to a rapamycin type derivative and an optical isomer and pharmaceutically acceptable salts thereof. The invention further relates to an application of the compound to preparing a medicine for treating and/or preventing cancers, and a preparation method of the rapamycin type derivative.
EP2044026A1 Method of treatment of glioma brain tumour The present invention relates generally to therapeutic agents, formulations comprising them and their use in the treatment, amelioration and/or prophylaxis of glioma brain tumours and related conditions. The therapeutic agent comprises two fused 6- membered rings with at least a nitrogren at position 1 and a hydroxyl at position 8.
US20120309761 Fast-response photochromic nanostructured contact lenses A bicontinuous microemulsion of water, a monomer, and a surfactant copolymerizable with the monomer is polymerized to form a polymeric material, the polymeric material comprising a polymer matrix defining interconnected pores. The polymeric material may additional comprise at least one photochromic agent. The photochromic agent may be dispersed in one or both of the polymer matrix or the interconnected pores. The polymeric material may be used to form photochromic articles including ophthalmic articles such as contact lenses.
CN102058524A Cyclophosphamide injection and preparation method thereof The invention relates to an injectable cyclophosphamide preparation and a preparation method thereof. The invention is characterized in that the preparation is composed of cyclophosphamide, water soluble filler, pH regulator, water for injection and osmotic pressure regulator, wherein the weight percent of the cyclophosphamide is 0.001-50%, and the balance is pharmaceutical excipient or water. The injectable cyclophosphamide preparation prepared by the invention has good stability and high bioavailability, and the demand on injectable drug required for treating clinic acute and chronic granulocyte leukaemia is met.
WO2010117639A2 Inhibition of prostglandin e2 receptors for the treatment of endometriosis The present invention describes the selective inhibition of prostaglandin receptors (PGE2), e.g., EP2 and EP4, by one or more inhibitors are selected from 6-Isopropoxy-9-oxoxanthene-2-carboxylic acid and (4Z)-7-[(rel- l S,2S,5R)-5-((l,l '-Biphenyl-4-yl)methoxy)-2-(4-morpholinyl)-3-oxocyclopentyl]- 4-heptenoic acid and salts thereof as a potential therapeutic tool or to expand the spectrum of currently available treatment options for endometriosis and other chronic gynecological diseases in reproductive age women. PGE2 inhibition through novel cell signaling mechanisms identified by the present invention provides an effective and attractive therapeutic tool for treatment without compromising pregnancy and sex life in the women.
WO2010000817A1 Antitumoral macrolides Antitumoral compounds of general formula (I), wherein R1- R14 and the ------- lines take permitted meanings for use in the treatment of cancer.
CN101120958B Medicinal preparation for treating liver cancer and leukemia and producing technology thereof The present invention discloses a pharmaceutical preparation for liver cancer treatment and leukemia treatment as well as the production technology, which is characterized in that the pharmaceutical preparation comprises three chief herbs of the abrotani herbal oil, the glycyrrhetate and the Tretinoin, or single abrotani herbal oil, or the combination of any two herbs together with proper medicinal excipient formulation. The dosage form available for clinical application is prepared. Pharmacodynamic test proves that the medical preparation in the present invention possesses targeting effect to the tumor cells and the present invention can significantly inhibit the cell growth and proliferation of liver cancer, lung cancer and leukemia. The present invention can also greatly prolong the survival period of the mice with liver cancer or lung cancer. The medical preparation in the present invention possesses properties of stable and controllable quality, little toxic and side effects, reliable therapy effect. Name of the production preparation is FuErKang plus the formulation name, such as the FuErKang injection and the FuErKang oral liquid.
WO2010131717A1 Prion protein structure transformation inhibitor and utilization of same Provided is a novel compound which is capable of inhibiting the formation of an infectious prion protein via binding to a normal prion protein. Specifically provided is a compound represented by formula (1). In formula (1), X represents a carbon atom or a nitrogen atom; R1 and R2 may be either the same or different and represent a hydrogen atom, an oxygen atom, a halogen atom, a hydroxy group, a mercapto group, a cyano group, a carboxy group, a carbamoyl group, an alkoxycarbonyl group, an acyloxy group, an acyl group, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted amino group, etc.; and R3 to R6 may be either the same or different and represent a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, etc., provided that at least one of R1 and R2 represents a group other than hydrogen atom.
CN101134034A Immunological enhancement medicine and method for preparing the same The present invention relates to immunological promoter, and is especially one kind of pidaomode injection for intravenous dripping. The pidaomode injection is superior to available orally taken preparations, which have bioavailability likely to be reduced by diet. The pidaomode injection is prepared with pidaomode in 0.2-0.8 weight portions, and pharmaceutically acceptable carrier or excipient in 0-2.0 weight portions.
US20090281040 Methods For Treating Endoplasmic Reticulum (ER) Stress Disorders The present invention provides methods for treating ER stress disorders and for identifying compounds for treating ER stress disorders.
EP1274459B1 Sustained release formulations comprising growth hormone This invention provides sustained release preparation of growth hormone, especially human growth hormone.
CN101606930B Application of pseudolaric acid B and derivative thereof in preparation of immunity inhibitor The invention discloses a pseudolaric acid B and the application of derivative thereof in the preparation of immunity inhibitor. Experiments prove that the pseudolaric acid B and the derivative thereof have excellent immunity inhibiting effect and lower toxicity, so that the pseudolaric acid B and the derivative thereof or pseudolaric acetate and salt of the derivative of the pseudolaric acid B can be taken as medicine for preventing or treating exclusive reaction, autoimmune disease, inflammatory disease, allergic disease and the like which are related to immunity and caused by organ or skingrafting of mammal (especially human beings).
US20110166163 Substituted furopyrimidines and use thereof The present application relates to novel substituted furopyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases.
CN101759749A Ginsenoside Rg 1 containing ginsenoside Rf and/or pseudo-ginsenoside F11 impurity The invention discloses standard effective ingredients of ginsenoside Rg 1, which is characterized by comprising the ginsenoside Rg 1 the content of which is more than or equal to 90% and less than 100%, wherein, the content of ginsenoside Rf and/or pseudo-ginsenoside F11 impurity is more than or equal to 0.05% and less than or equal to 5%; or the content of the ginsenoside Rf and/or pseudo-ginsenoside F11 impurity is more than or equal to 0.1% and less than or equal to 5%; or the content of the ginsenoside Rf and/or pseudo-ginsenoside F11 impurity is more than or equal to 0.5% and less than or equal to 5%. A pharmacological test proves that the standard effective ingredients of the invention have good pharmacological action, and the main ingredients have synergistic effect with the impurity, thus the ginsenoside Rg 1 can be taken as raw materials in pharmaceutical preparation.
US7329761 Substituted imides Novel imides are inhibitors of tumor necrosis factor alpha and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is (R)-2-Phthalimido-3-(3′,4′-dimethoxyphenyl)propane
CN1899285A Mycoporin vaginal soft capsule and its preparing method The present invention relates to soft mycosporin capsule for vagina and its preparation process. Each of soft mycosporin capsules contains mycosporin in 50-300 mg and medicinal supplementary material vaseline and paraffin, and the capsule shell contains gelatin in 10 weight portions and glycerin in 4.0-5.5 weight portions. The preparation process includes the steps of dissolving gelatin in water and adding glycerin and proper amount of preservative, vacuum deairing, mixing mycosporin and medicinal supplementary material, and pressing into soft capsule. Compared with available mycosporin preparation forms, the soft mycosporin capsule has the advantages of stable quality, convenient carrying and administration, and fast leaching of the effective components.
CN102068424A Brain atrophy treating medicament prepared from active ingredient of radish seed The invention discloses a senile dementia treating medicament prepared from an active ingredient of radish seed. A method for preparing the medicament comprises the following steps of: crushing the radish seed serving as a raw material; performing solvent extraction or solvent system extraction; deionizing with ion-exchange resin; purifying by using an ultrasonic standing wave liquid-phase preparative chromatography; and mixing the radish seed and a proper excipient to prepare tablets or slow release capsules. The medicament has the advantages of wide raw material resource, rational process, controllable quality, low energy consumption and good clinic curative effect, and is suitable for industrial production.
WO2009154739A3 Smoothened receptor modulators The present invention relates, in general, to the Smoothened receptor and, in particular, to a method of modulating Smoothened receptor activity and to compounds and compositions suitable for use in such a method.
CN101346149A Ultrasonic cancer treatment enhancer and cell killer To provide an ultrasonic cancer therapy accelerator, or cytotoxic agent, that while ensuring high safety, can strikingly enhance the efficacy of ultrasonic cancer therapy. There is provided an ultrasonic cancer therapy accelerator, or cytotoxic agent, comprising metal semiconductor particles. The ultrasonic cancer therapy accelerator or cytotoxic agent upon ultrasonic irradiation is activated so as to achieve annihilation or destruction of cancer cells.
CN102920702A Dihydroartemisinin and Chinese blister beetle composition, enteric preparation and application and preparation thereof The invention relates to a dihydroartemisinin and Chinese blister beetle composition, an enteric preparation and an application and a preparation thereof. The composition mainly comprises the materials in part by weight as follows: 5-20 parts of dihydroartemisinin, 0.1-0.5 parts of sodium cantharidate and 5-15 parts of vitamin B6. The enteric preparation comprises a chip and an enteric coating. The composition and auxiliary materials are prepared into the chip and the enteric coating to obtain the enteric preparation. The dihydroartemisinin and Chinese blister beetle composition and the enteric preparation prepared treat cancers and improve immunity, and have good curative effect in treatment of various cancers such as cancer of the liver, lung cancer and ovarian cancer and the like. The enteric preparation releases medicines in the intestinal tract, avoids stomach irritation and toxicity, and improves the absorptivity.
US7056938 Method for scavenging radicals with urocanic acid, derivatives and analogues Upon exposure to UVB, the epidermal component trans-urocanic acid is not only photoisomerized into cis-urocanic acid, but will also, at least in part, be photooxidized into urocanic acid oxidation products. We hypothesized that urocanic acid oxidation products can mimic UV-induced systemic immunosuppression comparable to the suppressive properties already established for cis-urocanic acid. A crude mixture of urocanic acid oxidation products showed a significant suppression of the sensitization phase of the systemic contact hypersensitivity response to picryl chloride. Three of the urocanic acid oxidation products were selected for this study: imidazole-4-carboxylic acid, imidazole-4-carboxaldehyde and imidazole-4-acetic acid. Effects on the sensitization-, elicitation- and post-elicitation phase of contact hypersensitivity to picryl chloride in BALB/c mice were studied and compared to the effects of cis-urocanic acid. Imidazole-4-carboxaldehyde was equally effective at suppressing the sensitization phase as cis-urocanic acid. The triplet combination of the imidazoles showed more pronounced suppression than that induced by cis-urocanic acid. The most effective compounds for the suppression of the elicitation phase appeared to be imidazole-4-acetic acid and cis-urocanic acid. Significant suppression of the post-elicitation phase was only obtained with the triplet combination of imidazole-4-carboxaldehyde, imidazole-4-carboxylic acid and imidazole-4-acetic acid, which combination appeared to be effective at all three tested phases, Because these three urocanic acid oxidation products are present in UVB-exposed human stratum corneum, these compounds may play a role in UVB-induced immunosuppression.
US20080051403 Treatment For Alzheimer's Disease And Related Conditions This invention provides the combination of a growth hormone secretagogue and a p38 kinase inhibitor for use in treatment or prevention of a disease associated with deposition of Aβ in the brain.
US20080166433 Methods and Composition For Dietary Supplements Compositions and methods are provided to reduce glucose concentration in an organism. Particularly contemplated compositions include a compound that binds to a thaumatin-like protein and that is isolated from a plant. Contemplated compositions further reduce blood lipid concentrations at the concentration effective to reduce the glucose concentration.
WO2013102897A1 Polymorphs of perampanel The present invention provides novel crystalline forms of perampanel, pharmaceutical compositions comprising same, methods for their preparation and uses thereof for treating seizures and epilepsy.
US20110092555 Thiazolidinedione compound A compound which is 5-{4-[(6-methoxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzyl}thiazolidine-2,4-dione hydrochloride, in crystal form wherein a powder x-ray diffraction pattern obtained by irradiation with a Cu Kα line shows main peaks at interplanar spacings d=14.29, 7.12, 5.34, 4.97, 4.74, 3.95, 3.85, 3.75, 3.55, 3.51, 3.15, 2.84, 2.76, 2.52 and 2.37.
US7250182 Medicament containing Epimedium extract for treatment of prostatic hyperplasia and prostatitis This present invention relates to a method for extracting Epimedium herb to prepare flavones and polysaccharides combinations in which their ratios vary from 2:8 to 8:2 by weight and applying these extracted compositions in treatment of prostatic hyperplasia. Total flavones of the extracts are in the range of 20-90% and the molecular weights of extracted polysaccharides vary from 1,000 to 700,000 Daltons. This invention also includes a method for preparing compounded formulations which contain extracts of Radix Ginseng, pollens, Radix Astragali, Cortex Phellodendri, Epimedium flavones and polysaccharides and administering these compositions directed at treatment of prostatic hyperplasia and prostatitis. Clinical study has showed that these extracts and formulations are effective in treatment of prostate illness with no adverse reactions.
WO2007107442A3 Bis1,2,3,4-tetrahydroisoquinoline derivatives and their uses as pharmaceuticals Use of Bis 1,2,3,4-tetrahydroisoquinoline derivatives represented by formula (I) as SK channel blockers and for the preparation of a medicament useful for the treatment of disorders of the central nervous system.
US7887841 Multilayer, drug core, delay release gum compression coatings A chronotherapeutic pharmaceutical formulation comprising a core containing an active agent (e.g., a drug) and a delayed release compression coating comprising a natural or synthetic gum applied onto the surface of the core.
CA2142280C Metal-mediated cross-coupling with ring-metalated porphyrins Porphyrins substituted with, for example, vinyl and acetylene groups are provided, along with polymers containing the same. In preferred embodiments, the substituted porphyrins are prepared by coupling halogenated porphyrins with anionic groups via metal-mediated cross-coupling reactions under stoichiometric or catalytic conditions.
US20090118660 Apparatus and method for in-vivo plasmapheresis using periodic backlush containing anticoagulant Method for in-vivo plasmapheresis utilizing a plurality of elongated hollow microporous filter fibers periodically interrupt diffusion of blood plasma from a patient, and, for a selected time, directing backflush fluid into the fibers at a pressure and interval sufficient to cleanse the fiber pores, after which plasma diffusion is resumed. The backflush fluid, preferably a normal saline solution, may contain an anticoagulant such as heparin, citrate or NO donor in suitable concentration for systemic anti-coagulation or for treating the fiber for thromboresistance.
US20110268761 Effective Sensitizing Dose of a Gelled Immunomodulating Topical Composition The present invention relates to compositions and methods of treating warts and other human papilloma virus (HPV) skin infections. The present invention relates to compositions and methods of treating skin cancer.
US20120010168 Unique Dual-Action Therapeutics A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X═C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.
CN1715298A Ganodema tsugae-proteoglycan and its preparing method and use The present invention discloses a kind of crude Ganoderma tsugae proteoglycan product and three kinds of purified Ganoderma tsugae proteoglycan products and their preparation process and application in preparing antitumor resisting medicine. The crude Ganoderma tsugae proteoglycan product is mixture including three kinds of proteoglycan, P1, P2 and P3 with the weight ratio of P1 1.50-3.00 wt%, P2 52-58 wt% and P3 20-25 wt%. Their polysaccharide part is uniform glucosan with glucosidic bond of beta-(1-3) configuration. Of the proteoglycans, P1 has n number of 500-600 and molecular weight 180-220 KDa; P2 has n number of 42-69 and molecular weight 15-25 KDa; and P3 has n number of 17-34 and molecular weight 6-12 KDa. Their protein part is combined to the reduction end of the polysaccharide part in integral form.
US20080004284 Method for treating fibromyalgia syndrome and related conditions The present invention provides a method for treating certain rheumatic conditions such as fibromyalgia syndrome, chronic fatigue syndrome, myofascial pain syndrome, and Gulf War syndrome, among others, by administration of trimetazadine, along with related compositions and kits.
EP1061873B1 Use of glyceraldehyde as corneal hardening agents An Enzyme Orthokeratology method is provided for correcting refractive errors in the eye of a subject mammal. Accelerating reshaping of the cornea is accomplished by administering a corneal hardening amount of a corneal hardening agent to the eye of the subject. Reformation is accomplished under the influence of a rigid contact lens or a series of lenses having a concave curvature that will correct a refractive error. The cornea rapidly reshapes its convex curvature to the concave curvature of the contact lens, rendering the eye emmetropic. The cornea is permitted to 'harden' to retain the new emmetropic shape. After 'hardening' has occurred, the lens rendering the eye emmetropic is removed.
US20120328537 Topical wound management formulation A topical wound therapeutic treatment provides a gel preparation of very low toxicity and good antimicrobial properties. The gel can be formulated for both intra-oral and extra-oral use. The preparation uses high concentration Xylitol in combination with other agents including a non-Xylitol, sugarless, antimicrobial sweetener, such as DL-Menthol, oil of Peppermint, Sorbitol and Glycerin to achieve rapid wound healing with comfort. The dried gel forms a water soluble occlusive dressing to promote healing.
CN101721697A Anti-cancer and anti-infectious disease compositions and methods for using same The present invention provides methods and compositions for treating and/or preventing cancer in a subject via administration of a non-pathogenic virus. The present invention also provides methods and compositions for treating and/or preventing infectious diseases in a subject via administration of a non-pathogenic.
WO2011050947A3 Tape, in particular, adhesive tape, for the treatment of skin disorders comprising at least one hyperkeratosis inhibitor and/or at least one keratinolytic agent The present invention relates to a tape for the treatment of skin disorders comprising at least one base layer having a first surface facing away from the skin during use and a second surface facing towards the skin during use, and at least one carrier layer on the side of said second surface, having a first surface facing away from the skin during use and a second surface facing towards the skin during use, which covers at least part of the second surface of said base layer and which comprises at least one hyperkeratosis inhibitor and/or at least one keratinolytic agent.
WO2013056679A1 Novel heteroaryl-amino derivatives Disclosed is a compound of formula (I), wherein R1, R2, L, Rm and Rn are as defined herein. The compound of formula (I) may be used in preventing and/or treating acyl CoA-diacylglycerol acyltransferase 1(DGAT-1) related diseases, such as obesity, coronary disease, hypertension, hyperlipidemia, arteriosclerosis, type II diabetes, stroke, hepatitis C, and the like.
CN101966166A Capsule containing cefixime liposome and preparation method thereof The invention relates to a cefixime liposome and a preparation method thereof as well as a capsule containing the cefixime liposome. The capsule comprises the cefixime liposome and a pharmaceutically acceptable vector, wherein the cefixime liposome is prepared from the following components in parts by weight: 1 part of cefixime, 1.25-5 parts of hydrogenated soybean lecithin, 1.25-5 parts of hydrogenated egg yolk lecithin, 1.25-10 parts of cholesterol and 0.1-2.5 parts of polysorbate 80. The capsule not only accords with the requirement on Chinese pharmacopoeia, but also has the advantages of stabler storage and rapider drug effect exertion and remarkably improved bioavailability compared with the common pharmaceutical cefixime pharmaceutical composition at a room temperature.
CN101835759A Arylindenopyrimidines and their use as adenosine A2a receptor antagonists This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses as an antagonist of Adenosine A2a receptors. Disorders treated ans/or prevented include Parkinson's Disease.
CA2186601C New combination of a .beta.-receptor blocker and a local anaesthetic New combination of a .beta.-receptor blocker, an enantiomer thereof, and a local anaesthetic, administered simultaneously or sequentially, giving excellent pain relief. Also comprised in the invention is the use of a non-selective .beta.-receptor blocker alone, especially a non-selective .beta.-receptor blocker giving pain relief.
US20100063152 Method and Topical Formulation for Treating Localized Edema Methods and formulations are provided for the treatment of localized edema, particularly localized edema resulting from chronic venous insufficiency. A metal ion sequestrant is topically administered to a subject afflicted with localized edema in combination with a permeation enhancer selected from methylsulfonylmethane and a combination of methylsulfonylmethane and dimethylsulfoxide. Topically administrable formulations for use in the aforementioned method are also provided.
CN101912547A Medicament for treating dizziness and preparation method thereof The invention discloses a medicament for treating dizziness, which is characterized by being prepared from the following raw materials in part by weight: 1 to 20 parts of rose, 1 to 20 parts of seville orange flower, 1 to 20 parts of ginger-processed bamboo shavings, 1 to 20 parts of ginger-processed pinellia, 1 to 20 parts of dried tangerine peel, 1 to 20 parts of Indian buead, 1 to 20 parts of mix-fried licorice, 1 to 20 parts of immature bitter orange, 1 to 20 parts of dried kudzuvine root, 1 to 20 parts of salvia, 1 to 20 parts of uncaria, 1 to 20 parts of raw magnetite and 1 to 20 parts of over 95 percent edible alcohol. The medicament can be absorbed through spleen and stomach by oral administration and absorbed through skin by external use, and can be compositely absorbed in a mode of combining the oral administration and external use. The medicament has the advantages of reasonable formula, simplified components, exact curative effect and treatment for both principal and secondary aspect of the disease. The invention also provides a method for preparing the medicament.
US7956047 Stimulating formation of collagen based extracellular matrix; fibrillogenesis agonism; wound healing The present invention comprises the use of chondroitin sulphate (CS-E) or an active fragment thereof for the treatment of diseases or conditions related to collagen fibril formation. Said compounds can be administrated either by oral, topical, injectable or by any other suitable route.
CN101632806B Medicinal composition, pill and preparation method thereof The invention provides a medicinal composition, which comprises the following raw materials: deer product, dodder seed, pyrite, white poria, milkwort, epimedium herb, malaytea scurfpea fruit, Chinese angelica, white paeony root, eucommia bark, cinnamomvine, ginger, acanthopanax bark, medlar, prepared rhizome of rehmannia, morindae root, radix astragali, scutellaria, fresh rehmannia root, cistanche, malt, medicated leaven, large-head atractylodes rhizome, tuber of multiflower knotweed, puncturevine fruit, beef back strap, liquorice root, fish fat and radix achyranthis bidentatae. The inventionprovides a pill and a preparation method thereof. The method comprises the mixing and shaping of an active component and accessory, wherein the active component is the medicinal composition provided by the invention. The medicinal composition provided by the invention can effectively improve the immunity of the human body and improve the sub-health.
DE102004044555A1 New modification of 2-indenylbutyric acid derivative, useful for treating e.g. diabetes and obesity, thermodynamically stable at room temperature Modification I of (2S)-2-((1S)-5-{2-[5-methyl-2-(4-methylphenyl)-1,3- oxazol-4-yl]ethoxy}-2,3-dihydro-1H-inden-1-yl)butyric acid (I) is new. Modification I of (2S)-2-((1S)-5-{2-[5-methyl-2-(4-methylphenyl)-1,3- oxazol-4-yl]ethoxy}-2,3-dihydro-1H-inden-1-yl)butyric acid of formula (IA) is new. An independent claim is also included for three methods for preparing modification I. [Image] - ACTIVITY : Antidiabetic; Anorectic; Antilipemic; Antiarteriosclerotic. No details of tests for these activities are given. - MECHANISM OF ACTION : None given.
WO2010030954A1 Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A1, A2, A3, A4, A5, A6, T1, T2, W, X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula (I).
CN103120737A Method for preparing ointment for treating acne The invention relates to the technical field of cosmetics, in particular to a method for preparing ointment for treating acne. The method for preparing the ointment for treating acne comprises the following steps of: grinding calomel, baikal skullcap root, angelica dahurica, giant typhonium rhizome and divaricate saposhnikovia root to obtain powder, mixing by using whitish honey, finally adding bee wax and dissolving, mixing and stirring, and cooling to obtain the ointment, namely a finished product. The method for preparing the ointment which has the strong functionality and can radically treat acne effectively is provided.
US6897316 Substituted 2-phenyl-4-quinolone-3-carboxylic acid compounds and their use as antitumor agents Substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives and their salts were synthesized. The results of preliminary screening revealed that these compounds are potent in killing solid tumor cancers.
CN103483275A Coupling compound of NSAID anti-inflammatory pain killers and EGFR kinase inhibitor and synthetic method and application of coupling compound The invention discloses a coupling compound or salt or a stereoisomer or prodrug molecules, which are pharmaceutically acceptable. The coupling compound of the structure shown in the formula I or II or III is formed by connecting NSAID anti-inflammatory pain killers and an EGFR kinase inhibitor through ester bonds, wherein the R is the NSAID anti-inflammatory pain killers. The coupling compound obtained by coupling the NSAID anti-inflammatory pain killers and the EGFR kinase inhibitor has the good cancer treatment effect, and the new drug is provided for clinic treatment choices.
US7767669 inhibitors of phosphatidyl inositol (PI) 3-kinase, such as 4-(1H-indazol-5-ylamino)-6- (4-methoxy-3- methylphenyl)-2-morpholin- 4-ylpyrimidine-5-carboxylic acid, used for the treatment of breast cancer Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.
US7189749 Substituted phenoxyacetic acids Disclosed are substituted phenoxyacetic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds, alone or in combination with other therapeutic agents, and methods of treatment employing the compounds and pharmaceutical compositions, as well as methods for their synthesis.
US20050203155 Imidazole compounds and human cellular proteins casein kinase I alpha, delta and epsilon as targets for medical intervention against Hepatitis C Virus infections Novel imidazole compounds particularly useful against Hepatitis C Virus infections and diseases associated therewith are described. Applications of the human cellular proteins casein kinase I alpha (α), delta (δ), and epsilon (ε) as targets for medical intervention against Hepatitis C Virus (HCV) infections and diseases are also described. This invention further refers to a method for identifying compounds useful for the prophylaxis and/or treatment of Hepatitis C Virus infections and diseases, methods for treating Hepatitis C Virus infections and diseases, as well as pharmaceutical compositions useful for the prophylaxis and/or treatment of Hepatitis C Virus infections and diseases. Moreover, disclosed are antibodies, oligonucleotides and specific compounds which are effective for the detection, prophylaxis and/or treatment of Hepatitis C Virus infections and diseases. Solid supports useful for the identification of compounds suitable for preventing and/or treating Hepatitis C Virus infections and diseases are also disclosed.
US20080131521 Methods for Preventing or Treating Bone Disorders The present invention relates to a method of preventing or treating a bone disorder in a mammal, comprising administering to the mammal a therapeutically effective amount of a peptide having ability to modulate lipid metabolism but having no appreciable effect on IGF-1.
WO2009090023A1 Crystalline form i of ortataxel The present invention relates to an anhydrous, non-solvated crystalline form of Ortataxel (I) herein referred to as Form (I). This form is characterized by very low tendency to absorb humidity, ease of isolation and prolonged chemical and physical stability. Therefore, it can be advantageously used for the preparation of pharmaceutical compositions for the treatment of cancer.
WO2006103120A3 New heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-alzheimer agents The invention is related to compound which comprises at least one radical C=Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C=Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.
CN103446072A Palonosetron solid medicine composition The invention relates to a palonosetron solid medicine composition. The palonosetron solid medicine composition comprises palonosetron or a pharmaceutically acceptable salt and a pharmaceutically acceptable excipient of the palonosetron, and the solid medicine composition does not contain an adhesion agent.
EP1026945B1 Improved iodine antimicrobial compositions containing nonionic surfactants and halogen anions Stable, aqueous, iodine-based germicidal compositions are provided which include respective amounts of available iodine, non-ionic surfactant (e.g., polyoxyethylene, polyoxypropylene block copolymers) and an iodine-solubilizing halide ion selected from the group consisting of C1?- and Br-¿ and mixtures thereof. Use of C1- and/or Br- substantially reduces or completely eliminates the need for iodide ion in the compositions for maintaining available iodine in solution. The compositions can be in the form of dilutable concentrates or final use solutions.
CN102068414A Levetiracetam sustained-release tablets and preparation method thereof The invention discloses levetiracetam sustained-release tablets and a preparation method thereof. The levetiracetam sustained-release tablets consist of levetiracetam, a filler, a sustained-release agent, an adhesion agent and a lubricant according to the weight ratio of 100: 30: (3-60): (30-70): 1. The preparation method comprises the following steps of: pelletizing by the wet method, drying the granules, arranging the granules and adding a proper quantity of lubricant, uniformly mixing and pressing to obtain the levetiracetam sustained-release tablets. Compared with the common preparation, the levetiracetam sustained-release tablets prepared by the preparation method have the advantages of small blood concentration fluctuation range, reduction in toxin and side effect and increase in biddability of patients by oral administration once every day. The sustained-release preparation will be clinically applied to additional treatment on partial seizure of epilepsia patients.
WO2011151330A1 1-(2-fluorobiphenyl-4-yl)-cyclopropanecarboxylic acid derivatives for the therapy of prion diseases The present invention relates to the therapeutic use of derivatives of l-(2-fluorobiphenyl-4-yl)-cyclopropanecarboxylic acid for the prevention and/or treatment of prion diseases in animals and humans.
US20080004236 High Dose, Short Interval Use of Sulfated Polysaccharides for Treatment of Infections Methods and compositions for treating or preventing acute or chronic viral infection over a short time interval in mammals with sulfated polysaccharides wherein the polysaccharides have a percent of sulfur with respect to the sugar residue effective to enable maximal interaction of constituent sulfate groups with the microbe which causes the infection and wherein the sulfated polysaccharide is not substantially endocytosed or degraded by cell receptor binding in the mammal and thereby retains antiviral activity in vivo.
US7166307 Herb medicine composition to be spread on sanitary napkin for female The present invention relates to a Galla Rhois-containing composition to be spread on sanitary napkin for female. Preferably, the present invention further comprises one or more herb medicine selected from a group consisting of Artemisia Folia, Sophorae, flavescens, Phellodendri Cortex, Torilis anthriscus and alum.
US20100286630 Method For Treating Overactive Bladders And A Device For Storage And Administration Of Topical Oxybutynin Compositions The invention relates to a method for treating overactive bladders and a device for storing and administering non-occluded oxybutynin topical compositions.
CN103142520A Kelimycin tablet and preparation method thereof The invention relates to a kelimycin tablet and a preparation method thereof. The kelimycin tablet comprises kelimycin and a tablet core comprising pharmaceutically acceptable adjuvants; and the pharmaceutically acceptable adjuvants include microcrystalline cellulose, carboxymethyl starch sodium, povidone K30 and magnesium stearate. The preparation method comprises the following step of: preparing the medicated tablet core, wherein an inside and outside addition method is adopted for the carboxymethyl starch sodium in the preparation of the medicated tablet core. The kelimycin tablet disclosed by the invention has the advantages of faster disintegration and better dissolution rate, and is easy to granulate. The preparation method of the kelimycin tablet has the advantages of simple process, large production quantity and low production cost, and easily realize hygienic standard and is suitable for large-scale mechanized production.
CN102335183B Application of bidens bipinnata polyacetylene as active component in bidens bipinnata to preparation of medicine for controlling acute liver injury The invention discloses a novel application of bidens bipinnata polyacetylene as an active component in bidens bipinnata, in particular the application of the bidens bipinnata polyacetylene to the preparation of a medicine for controlling acute liver injury. According to the invention, animal experiment is carried out to indicate that the bidens bipinnata polyacetylene can play a role of protecting a laboratory mouse with CCl4 induced acute liver injury; the bidens bipinnata polyacetylene has the capability of obviously reducing the levels of ALT (alanine aminotransferase) and AST (aspartate aminotransferase) in serum, reducing the content of MDA (malondialdehyde) of liver tissues, remarkably enhancing SOD (Superoxide Dismutase) and GSH-Px (Glutathione peroxidase) activities of the liver tissues, obviously reducing the content of NO in the liver tissues, and suppressing the expression of NF-kB (Nuclear factor-kappaB) of liver cells; and therefore, the bidens bipinnata polyacetylene has a more ideal prospect in the preparation of the medicines for preventing and treating the acute liver injury.
CN101396345A Sinomenine hydrochloride sustained-released injection and preparation method thereof The invention discloses a sinomenine hydrochloride sustained release injection and a preparation method thereof. The sustained release injection comprises one of synthetic polymer nanometer sinomenine hydrochloride sustained release injection, natural polymer material microsphere sinomenine hydrochloride sustained release injection, lipid sinomenine hydrochloride sustained release injection, multivesicular liposome sinomenine hydrochloride sustained release injection and gelatin sinomenine hydrochloride sustained release injection. Various sinomenine hydrochloride sustained release injections prepared by the invention by different methods can prolong the acting time of drug, reduce drug administration times, keep stable blood concentration in vivo and reduce the toxic and side effects of the drug.
CN101596244A External-use medicine for treating rheumatism rheumatoid arthritis The invention relates to an external-use medicine for treating rheumatism rheumatoid arthritis, which is prepared from the following components according by weight percent: 12 to 15% of radix aconiti, 12 to 15% of kusnezoff monkshood, 12 to 15% of ebony, 12 to 15% of honeysuckle flower, 12 to 15% of safflower, 12 to 15% of borneol, 12 to 15% of ural falsespiraea and 12 to 15% of radix sileris. The production method comprises the following steps: the eight kinds of medicines are selected and quantified according to matching, then are washed by cool boiled water, are put into a soaking vat, are added with 400 to 600 (parts by weight) of 50 to 70 degrees white spirit and are soaked at normal temperature for 7 to 10 days, wine liquor is filtered, and the obtained filter liquor is just the medicated wine. The use method comprises the following steps: external application is carried out for 1 to 2 times every day, the medicated wine is applied to an affected part every time, and then a hot towel is used for hotly compressing the affected part. The external-use medicine has no toxic or side effect, takes effect quickly after external application and has the effects of relaxing muscles and tendons, promoting blood circulation, alleviating pain, decreasing swelling, and the like, the effective rate to rheumatism rheumatoid arthritis is 100%, and the cure rate is 48%; and simultaneously, the external-use medicine also has a certain effect to periarthritis humeroscapularis and lumbar muscle strain.
US20100119587 Solid lipidic particles as pharmaceutically acceptable fillers or carriers for inhalation The present invention relates to new compositions of (active) solid lipidic particles (SLP), e.g. for inhalation, and their use as carriers or as fillers in pharmaceutical compositions. It also relates new formulations obtained by mixing a SLP composition of the invention and a (micronized) active compound. It further relates to a method for fabricating said compositions of (active) solid lipidic particles.
CN102908462A Isatis root particle and preparation method thereof The invention relates to an isatis root particle and a preparation method thereof. The isatis root particle is composed of 10-20 parts of isatis root, 10-15 parts of folium isatidis, 10-20 parts of dextrin, 2-5 parts of liquorice, 1-3 parts of honeysuckle, 0.1-0.5 parts of vitamin C and 0.1-0.2 parts of steviosin. The preparation method is that the isatis root, the folium isatidis, the liquorice and the honeysuckle are washed by clean water to be placed in a 60-80 DEG C drying oven for drying and smashing; an ethanol solution is added, and 120 W ultrasonic wave is used for extracting and centrifuging to obtain supernatant liquor; membrane filtration is carried out on the supernatant liquor, and decompression and concentration are carried out to obtain an extractive; and the extractive, vitamin, steviosin and dextrin are evenly mixed, and freeze drying is carried out after palletizing. The isatis root particle is rich in active ingredients, can be used for treating diseases such as tepidity fever, wind-heat type common cold, headache and dermexanthesis, and is good in curative effect, stable in quality and free of side effects.
US20120190646 Compositions Comprising Thalidomide and Artemisinin for the Treatment of Cancer The present invention relates to pharmaceutical compositions for the treatment of cancer and especially for the treatment of hematological malignancies such as multiple myeloma. Specifically, the present invention relates to pharmaceutical composition for the treatment of cancer comprising: thalidomide, or a derivative thereof, or salts or solvates thereof; one or more artemisinin compounds, or salts or solvates thereof; and one or more pharmaceutically acceptable carriers and/or excipients.
WO2011031561A2 Nucleic acid molecules and uses thereof Provided in this application are formulations of double stranded RNA molecules and Krebs Cycle analogs that improving ribonuclease stability, reducing off-target effects of a double stranded siRNA molecule, or of reducing interferon responsiveness of a double stranded siRNA molecule using such dsRNA. Also disclosed are methods of treating a primary tumor or a metastasis by contacting circulating tumor cells, a primary tumor, or a metastasis with a described formulation.
EP1101497B1 Stabilized oily preparations of tobicillin (beta-lactam antibiotic) Stabilized preparations which contain a β-lactam antibiotic having an esterified carboxyl group attached directly to the mother nucleus, an oil and a phosphate.
CN1589781A Compound amino phenol alkyl amine get agent and its production method A compound alkylamine aminophenate gel is prepared from compound alkylamine aminophenate powder, agar, cane sugar, soluble starch and water through proportionally mixing compound alkylamine aminophenate powder, soluble starch and water, stirring, and adding the solution of agar and cane sugar.
CN101429181A P-hydroxybenzene acrylic acid derivative and uses thereof The invention discloses a p-hydroxy phenyl acrylic acid derivative, which has a chemical structure expressed by general formula (I). The invention also discloses application of the p-hydroxy phenyl acrylic acid derivative to preparing COX-2 selective inhibitor medicament, and a pharmaceutical composition for treating and preventing pain, inflammation, rheumatoid arthritis, osteoarthritis or dysmenorrheal diseases, or antiviral and antibacterial pharmaceutical composition for treating and preventing virus and bacterial infection, or pharmaceutical composition for treating and preventing atherosclerosis, thrombosis, apoplexy or ischemia cerebrovascular diseases, wherein the pharmaceutical composition contains the p-hydroxy phenyl acrylic acid derivative or medicinal salt thereof with curative effective dose.
US7064120 For prevention and/or suppression of preterm labor, suppression of labor at term prior to caesarean delivery, and for the treatment of dysmenorrhea; useful in enhancing fertility rates This invention provides novel substituted tricyclic pyridyl carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea, endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.
US20100056447 Immunization against chlamydia pneumoniae The published genomic sequence of Chlamydia pneumoniae reveals over 1000 putative encoded proteins but does not itself indicate which of these might be useful antigens for immunization and vaccination or for diagnosis. This difficulty is addressed by the invention, which provides a number of C. pneumoniae protein sequences suitable for vaccine production and development and/or for diagnostic purposes.
CN102093274A Chalcone-containing acylthiourea compounds and preparation method and use thereof The invention provides chalcone-containing acylthiourea compounds and a preparation method and use thereof and belongs to the technical field of chemical synthesis. The compounds are prepared by reacting acyl chloride with ammonium thiocyanate in the presence of a phase transfer catalyst in a protonic solvent to obtain acylisosulfocyante, reacting acylisosulfocyante with aminoacetophenone to obtain N-benzoyl-N'-acetylphenylthiourea, and performing condensation of N-benzoyl-N'-acetylphenylthiourea and aromatic aldehydes under an alkaline condition to obtain target compounds. The chalcone-containing acylthiourea compounds prepared by the invention have carbonyl, vinyl, acyl and thiourea functional groups and belong to bioactive materials having multiple functional groups. Initial bioactivity tests show that the materials have regulating effect on the growth of dicotyledonous rape seeds.
EP2672971A1 Metabotropic glutamate receptor group i antagonists for treatment of abnormal union of tissue Use of a metabotropic glutamate receptor group I antagonist, or a pharmaceutically acceptable salt, prodrug or an optical isomer thereof, for the manufacture of a medicament for the treatment or the prevention of abnormal union of tissue, is provided. A related method is also provided.
WO2013154373A1 Composition comprising purine derivatives or salt thereof for preventing or treating atopic dermatitis Provided is a composition for preventing or treating atopic dermatitis, comprising 2-amino-1,9-dimethyl purine-6-one or a pharmaceutically acceptable salt thereof as an active ingredient. Further provided is a cosmetic composition comprising 2-amino-1,9-dimethyl purine-6-one or a pharmaceutically acceptable salt thereof for improving atopic dermatitis. Also provided is a food (i.e. a functional food) comprising 2-amino-1,9-dimethyl purine-6-one or a pharmaceutically acceptable salt thereof for preventing or improving atopic dermatitis.
US20120301537 LIPOSOME CONTAINING shRNA MOLECULE TARGETING A THYMIDYLATE SYNTHASE AND USE THEREOF This method provides a method for delivering shRNA targeting TS in vivo. In addition, the following is provided: an antitumor agent, which comprises short hairpin RNA (shRNA) capable of inhibiting expression of thymidylate synthase by RNAi action and a PEG-modified cationic liposome, wherein the shRNA is bound to the surface of the PEG-modified cationic liposome and has an overhang comprising at least two nucleotides at the 3′ end.
CA2408323C Drug delivery systems for photodynamic therapy The invention is generally related to the field of photodynamic therapy by use of photosensitizers and stabilized formulations of the photosensitizers. These formulations may be used to deliver a photosensitizer as a pharmaceutical, agricultural, or industrial agent. The photosensitizer containing formulations and compositions of the invention comprise one or more block copolymers. Furthermore, the invention relates to processes for the production of, and application of, said formulations and compositions as photosensitizer drug delivery systems.
WO2012159565A1 6-(aryl-carboxamide) imidazo [1,2-a] pyrimidine and 6-(aryl carboxamide) [1,2,4] triazolo [4,3-a] pyrimidine as hedgehog pathway inhibitor and use thereof Provided are new 6-(aryl-carboxamide) imidazo [1,2-a] pyrimidine and 6-(aryl carboxamide) [1,2,4] triazolo [4,3-a] pyrimidine as represented by formula I. Ar, A, and R2-R4 are as defined in the present application. The compound represented in formula I is a Hedgehog pathway inhibitor. Hence, the compound of the present invention can be used for treating diseases caused by abnormal Hedgehog activity, such as cancers.
CN103263414A Application of 2,2'-(1,4-phenylene)di(benzimidazole-5-carboxylic acid) in preparation of antitumor drug The invention discloses applications of 2,2'-(1,4-phenylene)bi(benzimidazole-5-carboxylic acid) shown as a chemical structural formula I with a good inhibitory activity on human cervical carcinoma cells (Hela cells), human hepatoma cells (Bel 7402 cells) and human lung adenocarcinoma cells (A549 cells) in the preparation of drugs anti-human cervical cancer, anti-human liver cancer, and anti-human lung adenocarcinoma.
WO2014043368A1 Methods for increasing brain functionality using 2-fucosyl-lactose Disclosed are methods for enhancing learning and/or memory, enhancing memory acquisition, memory retention and recall by inducing a higher long-term potentiation in hippocampal neuronal synapsis in individuals. The methods include administration of 2-fucosyl-lactose to an individual.
US20080081070 Pharmaceutical formulation with enhanced solubility for the delivery of corticosteroids Formulations have been developed to improve the solubility of corticosteroids such as fluticasone proprionate in a composition designed to achieve localized release of the drug in the small intestine and/or colon. In one embodiment, solid dispersions of fluticasone are prepared wherein the drug is blended with or coated onto a highly water soluble substrate such as nonpareil (sugar beads) then coated with a layer of polymer soluble in small intestinal fluid, then coated with an enteric coating. The inner polymer layer controls release of the drug, and the enteric coating, a pH sensitive polymer that is broken down in the ileum and colon, controls localized release of drug at various sites within the gastrointestinal tract. The multilayer pharmaceutical composition can be in the form of pellets, tablets compressed from pellets or pellets packed into capsules. The release profile of the drug can be manipulated by (1) altering size or shape (i.e., surface area) and solubility of the inert substrate; (2) the ratio of drug to polymer, the polymer composition and solubility, the porosity of the polymer; (3) the drug form (i.e., free base or salt, or which salt); and the thickness and/or surface area of the drug/polymer and/or enteric coating. In a preferred embodiment, the composition is administered orally. This may also be packaged to provide for an escalating or tapering dosage.
CN103610659A Allicin medicinal composition and preparation method thereof The invention relates to an anti-dental-ulcer allicin medicinal composition and a preparation method thereof. The allicin medicinal composition is divided into two layers, which are respectively a medicine-containing adhesive layer and a waterproof protective layer, wherein an allicin cyclodextrin inclusion compound is prepared from allicin and cyclodextrin or derivative thereof in the medicine-containing adhesive layer, so that the solubility and stability of allicin can be improved; the content of allicin is 0.1-2 percent of the weight of the composition. According to the two-layer composition, solution of the medicine to the opposite side of the oral mucosa and two-way adhesion of a tablet between the gum and the oral mucosa can be reduced, and the medicine is concentrated in the affected part, so that the drug effect is improved. The allicin medicinal composition prepared by the method has the advantages of reliable quality, stable property and good curative effect.
CN102552165A Sarpogrelate hydrochloride sustained release pellet and preparation method thereof The invention belongs to the field of medicinal preparation and discloses a sarpogrelate hydrochloride sustained release pellet and a preparation method thereof. The pellet is prepared by coating a sustained release coat on a medicine contained pellet core, wherein the formula of the medicine contained pellet core comprises the following raw materials in parts by weight: 75-100 parts of sarpogrelate hydrochloride and 0-25 parts of excipient, wherein the total weight part of the sarpogrelate hydrochloride and the excipient is 100 or the weight parts of the sarpogrelate hydrochloride and the excipient are increased or reduced by the same ratio; a surfactant accounts for 0.1-8% of the total weight of the sarpogrelate hydrochloride and the excipient; and a wetting agent accounts for 0.1-30% of the total weight of the sarpogrelate hydrochloride and the excipient. By using the preparation method disclosed by the invention, the medicine contained pellet core with low friability, higher yield, smaller particle size and smooth surface can be obtained; the pellet core is convenient to be further processed; according to the invention, the medicine contained pellet core is coated with the sustained release coat so as to obtain a potassium citrate sustained release pellet; and the pellet has the advantages of controllable and stable quality in vitro and sustained release characteristics in vivo.
CN101012210B Taxone derivatives, preparing method and pharmaceutical use thereof The invention discloses a new taxone derivant with formula (I), which is characterized by the following: adopting mother core of Paclitaxel or polyene Paclitaxel as central frame; introducing formyloxy on the C-13 lateral chain N and at least one taxone derivant substituted by methyl on the C1'' lateral chain in connection with formyloxy directly or carbon atom with chirality on the C1'' in connection with formyloxy directly; possessing at least one taxone chiral derivant substituted by methyl on the C1'' lateral chain.
CN103446057A Oral curcumin nano-granule and preparation method thereof The invention belongs to the technical field of pharmaceutical preparation and particularly relates to an oral curcumin nano-granule and a preparation method thereof. The nano-granule is prepared by self-assembling a ternary conjugated compound which is obtained by connecting taurocholic acid, heparin and curcumin through amido bonds, the curcumin is a core of the nano-granule, and the hydrophilic taurocholic acid is on the surface of the nano-granule. The oral curcumin nano-granule overcomes the poor water solubility of curcumin, the absorption of the nano-granule can be enhanced by utilizing the interaction of taurocholic acid and bile acid transporter of small intestine, the defect that the bioavailability of the oral curcumin is low can be overcome, and the heparin also has anti-thrombosis and anti-angiogenesis effect.
US20130029947 Progesterone containing oral dosage forms and kits The present invention provides for progesterone containing pharmaceutical oral dosage forms, pharmaceutical kits, and related methods. In one embodiment, an oral dosage form formulated for on-going administration is provided. The oral dosage form includes an amount of progesterone and a pharmaceutically acceptable carrier. The oral dosage form is formulated such that upon single dose administration to a non-pregnant woman in follicular phase, the oral dosage form provides a serum progesterone C24h of at least 0.20 ng/mL.
CN102871960A Lentinan injection and preparation method thereof The invention relates to a lentinan injection and a preparation method thereof. The lentinan injection comprises lentinan, sodium hydroxide, sodium dihydrogen phosphate and water for injection. The lentinan injection prepared according to the invention has the advantages of high storage stability and high compatible stability.
US20100129378 Treatment and diagnosis of abnormal bone density with an inhibitor of the glypican-sclerostin interaction Compositions and methods of treatment for abnormal bone density are disclosed based upon the finding that sclerostin must be bound to glypican in order to inhibit bone deposition. Methods for identifying agents that inhibit the glypican-sclerostin interaction are disclosed for treatment of bone deposition disorders. Diagnostic methods are also disclosed.
US20100216783 Compositions, synthesis, and methods of utilizing arylpiperazine derivatives The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.
CN102018700A Pharmaceutical preparation containing silymarin and preparation thereof The present invention discloses a pharmaceutical preparation containing silymarin, comprising the following components, by weight, 1 part of silymarin, 0.05 to 1.0 part of polyvinylpyrrolidone, 0.1 to 1.0 part of sugar alcohol, 0.1 to 1.0 part of microcrystalline cellulose, 0.005 to 0.05 part of nonionic surfactant, and the pharmaceutical preparation containing silymarin can be granules, capsules or tablets. The preparation method of the pharmaceutical preparation containing silymarin is further disclosed, comprising: dissolving silymarin using a solvent, adding some auxiliary materials and uniformly mixing them to give a homogeneous solution, adding the homogeneous solution to auxiliary materials to prepare granules capable of being filled into capsules, and then preparing tablets by further mixing with some auxiliary materials. The pharmaceutical preparation containing silymarin has high dissolution and bioavailability, and can be easily absorbed after oral administration.
WO2009132136A1 Carboxamide compounds for the treatment of metabolic disorders Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
CN1951389A Composition of Essentiale Phospholipids injection and preparation method thereof The invention relates to a compound of phosphatide bilineurine powder injection and relative preparation. Wherein, the inventive product can avoid benzenemethanol, to be stably used. And its components contain phosphatide bilineurine, cholate and support agent. The invention uses special method and treatment. The inventive product via frozen and dried is made into white or yellow powder injection, which can be diluted before vein injection.
CA2180010C 7-¬carboxyalkyl or alkenyl|-6-¬alkyl or alkenyl| 3-oxo-2,4-dioxobicyclo-¬3.2.1| octane and derivatives thereof The present invention relates to 7-[carboxyalkyl or alkenyl]-6-[alkyl or alkenyl]-3-3-oxo-2,4-dioxobicyclo[3.2.1] octanes and derivatives thereof. In particular, hydroxyl, nitro, amino, amido, azido, oxime, thiol, ether and thiol ether derivatives of said carboxy group are contemplated. In particular, 7-[6-carboxy-2-hexenyl]-6-[3-hydroxy-1-octenyl] of 3-oxo-2,4-dioxobicyclo-[3.2.1] octane and derivatives thereof are disclosed. These compounds are useful as ocular hypotensives and as (a) thromboxane mimetics for the prevention of hemorrhaging as follows: during surgery; tooth extraction; hemorrhaging associated with gastro-intestinal diseases and conditions such as hemorrhoids, inflammatory bowel diseases and gastric and peptic ulcers, as a result of stroke; as a complication in retinal diseases resulting in impaired vision and associated with menstruation, childbirth and uterine dysfunction and (b) selective vasoconstrictors for treating systemic hypotension, e.g. in restoring normal blood pressure in hemorrhagic, anaphylactic or septic shock victims, to provide local anti-inflammatory effects in the eye, skin and nose; to limit plasma exudation in burns, etc, and optimizing blood-born delivery of drugs and diagnostics in encapsulating vehicles.
CN100998575B Finger nail coating agent of antifungal agent and its preparing method An antifungal filming agent for finger nail contains antifungal imidazole medicine, antifungal acrylamine medicine, and a filing material chosen from PVC, ethylcellulose, carfopol resin, chitosan, acryl resin and polylactic acid. Its preparing process is also disclosed.
US20080009459 Methods of reducing papillomavirus infection using immunomodulatory polynucleotide sequences The invention provides methods for the treatment of papillomavirus infections. A polynucleotide comprising an immunstimulatory sequence is administered to an individual who has been exposed to or infected by papillomavirus. The polynucleotide is not administered with papillomavirus antigen. Administration of the polynucleotide results in amelioration of symptoms of papillomavirus infection.
US20120149663 Boronic acid compositions and methods related to cancer Disclosed are compounds and methods related to boronic acid derivatives of resveratrol. Certain of these derivatives have enhanced efficacy relative to resveratrol, function as irreversible modulators, and act at the GI/S phase of the cell cycle.
US20120108605 O-glcnac transferase inhibitors and uses thereof The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.
CN101606946A Compound kanamycin sulfate injection liquid for pig and preparation method thereof The invention discloses a compound kanamycin sulfate injection liquid for a pig and a preparation method thereof, aiming at providing a compound kanamycin sulfate injection liquid which has fast effect for treating pant disease of the pig, addresses both the symptoms and root causes, reduces the time and dosage of taking drug and has convenient drug usage, and a preparation method with simple technique and easy implementation. Each 100L injection liquid comprises: 5 to 20 billion units of kanamycin monosulfate, 1 to 10kg of lincomycin hydrochloride, 0.1 to 2kg of doxofylline, 0.05kg of dexamethasone sodium phosphate, 0.2kg of sodium bisulfite, 0.01kg of EDTA-2Na, 10kg of dimethyl acetamide and the balance of water for injection. The injection liquid reasonably mixes usage of all the components by a plurality of types of drugs, has fast effect for treating pant disease of the pig, addresses both the symptoms and root causes, reduces drug resistance of pathogenic microorganism and leads the pig to accelerate restoring. Simultaneously, the compound kanamycin sulfate injection liquid has convenient use, and can achieve the treatment effect of a plurality of types of drugs.
US20070293540 for hepatitis C; histone deacetylase inhibitors; N-hydroxy-4-{[(naphthyl-carbonylamino]alkoxy}benzamides; anticarcinogenic agent; acute promyelocytic leukemia; cell-cycle arrest in late G1 phase or at the G2/M transition The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
US7196105 Which suppresses I-kappa-B-alpha phosphorylation through inhibition kinase activity and downregulating NF-kappa-B; antiproliferative agents All multiple myeloma cell lines examined showed constitutively active IκB kinase (IKK), IκBα phosphorylation and constitutively active NF-κB. Curcumin, a chemopreventive agent, suppressed constitutive IκBα phosphorylation through inhibition of IKK activity and downregulated NF-κB. Curcumin also downregulated expression of NF-κB-regulated gene products such as IκBα, Bcl-2, Bcl-xL, cyclin D1 and interleukin-6. Consequently, curcumin suppressed multiple myeloma cell proliferation and arrested cells at the G1/S phase of the cell cycle. Curcumin also induced apoptosis and chemosensitivity to vincristine. Overall, results presented herein provide a molecular basis for the treatment of multiple myeloma patients with this pharmacologically safe agent.
WO2014161891A1 Ingenol mebutate in combination with laser therapy for the treatment of hyperkeratotic skin lesions The invention relates to the treatment of actinic keratosis (AK) lesions using laser therapy followed by treatment with ingenol mebutate (e.g., PEP005 Gel).
CN102432490A Agomelatine crystal form D and preparation method thereof The invention relates to the crystal form D of agomelatine serving as an anti-depression medicament and a preparation method thereof. The crystal form is represented by using an X-ray powder diffraction map, an infrared map and a differential scanning thermal analysis map. The crystal form D disclosed by the invention has the functions of a melatonin receptor excitant, is a 5-hydroxytryptamine 2C receptor antagonist, can be used for treating depression, seasonal affective disorder, sleep disorder, cardiovascular pathology, biological clock regulation and the like, and is a medicament which can be used for treating depression.
CN101897720A Medicinal composition for treating respiratory disease The invention relates to a medicinal composition for treating respiratory disease, in particular to a medicinal composition with synergy for sucking administration of ambroxol hydrochloride and tetrabutyl phenolic aldehyde. A medicament is administrated by sucking and directly enters an air passage, so the suction rate is high, the local has high concentration, low using amount and low adverse reaction, and the medicament can effectively promote the discharge of sputum of a patient and remarkably improve the application compliance of the patient.
CN1568947A Bromhexine Hydrochloride drop pills and preparation method thereof The invention discloses a bromhexine hydrochloride drop pill prepared through ultramicro disintegration and drop pills manufacturing technique, which has the advantages of improving collapse and dissolving speed, dissolving out speed and degree, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use, oral or swallow administration, it has good compliance, thus is especially suitable for children, the elderly, bedridden patients and dysphagia patients.
CN1810254A New medicinal use of paeonidin The present invention provides the application of paeonidin in preparing medicine for promoting post-operational intestinal function and preventing post-operational intestinal adhesion.
CN103285157A Medicine for treating neutral/oily skin chilblain and manufacturing method thereof The invention belongs to the technical field of medicine chemical engineering, and particularly relates to a medicine for treating neutral/oily skin chilblain, which is characterized by comprising the following raw materials in parts by weight: 6-12 parts of chili powder with the fineness of less than 150 meshes, 3-7 parts of Span-80, 4-8 parts of beeswax, 0.5-1.5 parts of eugenol, 4-8 parts of methyl salicylate, 1-3 parts of sheep horn powder or ox horn powder or buckhorn powder with the fineness of less than 150 meshes, 8-12 parts of lanonol, 4-6 parts of propanediol, 70-90 parts of paraffin oil, 80-120 parts of distilled water and 0.5-1.5 parts of propyl p-hydroxy benzoate. The invention also discloses a manufacturing method of the medicine for treating neutral/oily skin chilblain. The medicine is suitable for treating neutral/oily skin chilblain, and can heal the chilblain quickly; the manufacturing method is simple and easy to master; the medicine is fragrant, and the patient does not have any uncomfortable feeling or untoward effect in the application period.
CN1814290A Multi-layer tablet containing calsium-path receptor retarder and ACE inhibitor, and preparing method This invention is a multilayer tablet contains calcium channel acceptor retarder and ACE inhibitor. Its feature is that it contains calcium channel acceptor retarder pleated sheet and ACE inhibitor pleated sheet. The calcium channel acceptor retarder pleated sheet contains levamlodipine or amoldipine or salt that can be accepted on pharmacy of them. The ACE inhibitor pleated sheet contains methylphenidate or its pharmacy accepted salt. They can be produced by normal medicine equipment, and preparation is easy, the multilayer tablet made can be quickly disintegrated, main medicine component can be quickly stripped, and its quality stability is good.
WO2011094657A3 Additives for chlorine dioxide-containing compositions Provided is a composition containing chlorine dioxide, a vehicle and at least one compatible additive, The composition optionally contains a compatible amount of a non-compatible additive. Methods of making and using the composition are also provided.
EP2066314A2 Use of theogallin for the treatment of mental concentration disorders, depression and dementia Theogallin, its derivatives, its metabolite quinic acid, the derivatives thereof, its metabolites or the pharmaceutically acceptable salts of said substances can be used for producing a drug for use in the prophylaxis or treatment of neurological and psychiatric diseases of the central nervous system, especially of dementia such as Alzheimer's disease or Parkinson's disease, of depressions and concentration disorders such as attention deficit hyperactivity disorder.
US20120014964 Alpha synuclein toxicity Present inventions demonstrates that alpha synuclein toxicity such as α-synuclein mediated cell death, alpha synuclein induced reactive oxygen species (ROS) in a cell requires the proapoptotic endonuclease G and that the deletion of the endonuclease G or suppressing of the endonuclease G apoptotic pathway attenuates or counteracts such alpha synuclein toxicity. The present invention compositions and methods for inhibition of α-synuclein toxicity. The inhibiting α-synuclein toxicity can be used in methods of treatment of synucleinopathies, such as Parkinson's disease (PD), dementia with Lewy bodies (DLB), pure autonomic failure (PAF), and multiple system atrophy (MSA) and the manufacture of medicaments for such treatment. In particular The subject matter provided in herein relates to a pharmaceutical compositions containing inhibitors of endonuclease G, and their use in the treatment of synucleinopathies, such as Parkinson's disease, dementia with Lewy bodies, pure autonomic failure, and multiple system atrophy and the manufacture of medicaments for such treatment. Furthermore the present invention relates to a method for the identification of compounds attenuating the synuclein toxicity, said method comprising evaluating the inhibitory action of said compound on the endonuclease G dependent apoptosis.
EP1720826A2 Heteroalkyl-substituted biphenyl-4-carboxylic acid arylamide analogues Heteroalkyl-substituted biphenyl-4-carboxylic acid arylamide analogues are provided, of the formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
US20130039979 Medication on the basis of 3,3'-diindolylmethane (dim) with high-bioavailability and its use in treatment of human hyperplastic and inflammatory diseases The invention relates to medicine and chemico-pharmaceutical industry. A medication for treating human hyperplastic and inflammatory diseases containing 3,3′-diindolylmethane as an active agent and a carrier containing a mixture of cod-liver oil and at least one polysorbate at the following proportions of the components in mass %: 3,3′-diindolylmethane 1-20 cod-liver oil 10-20 polysorbate the balance.
US20100256187 Composition of 2,4,6- trifluoro-n-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-benzamide The present invention relates to discloses a pharmaceutical composition of 2,4,6-trifluoro-N-[6-(1-methyl-piperidin-4-ylcarbonyl)-pyridin-2-yl]-benzamide and a pharmaceutically acceptable carrier.
US20090023715 Wound Healing A phenothiazinium compound, compositions and medicaments for use in promoting wound healing and a method for promoting wound healing or cosmetic use by applying or administering a phenothiazinium compound to a wound site or the skin, and optionally exposing the wound site or skin to light.
WO2005023777A1 Ppar-activating compound and pharmaceutical composition containing same Disclosed is a compound for selectively activating PPAR α which is represented by the following general formula (1): (1) (wherein R1 and R2 may be the same or different and represent hydrogen atoms or the like; R3a, R3b, R4a and R4b may be the same or different and represent hydrogen atoms or the like; X represents an oxygen atom or the like; Y represents an oxygen atom, S(O)l group (l is a number of 0-2), carbonyl group, carbonylamino group, aminocarbonyl group, sulfonylamino group, aminosulfonyl group or NH group; Z represents CH or the like; n is a number of 1-6; and m is a number of 2-6), or a salt thereof. Also disclosed is a pharmaceutical composition containing such a compound.
EP1911746B1 The substance having antioxidant, geroprotective and anti-ischemic activity and method for preparing thereof The invention relates to the field of medicine, namely to new biologically active compounds, particularly to 2,4,6-trimethyl-3-hydroxypiridine derivatives and salts thereof (compound 1), having antioxidant, geroprotective and anti-ischemic action. The salts of compound (1) are prepared by reacting equimolecular quantities of 2,4,6-trimethyl-3-hydroxypiridine and dicarboxylic in solution of the lower spirit at the temperature of 60-100°C with following processing of the reactionary bulk by organic solvent and incubating within 2-5 h at 10-15°C.
WO2014082935A1 Cyclic nucleoside derivatives and uses thereof A compound of Formula (I) is provided that has been shown to be useful for treating a disease caused by a viral infection wherein R1, R2 and R3 are as defined herein.
WO2008129129A1 Heterocyclic phenyl carbamates as novel faah-inhibitors Fatty acid amide hydrolase inhibitors of the Formula (I) are provided, wherein R is a heterocyclic or heterocyclic carbonyl moiety and R' is a group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl. Pharmaceutical compositions and methods comprising compounds of Formula (I) may be used for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, anxiety, epilepsy, depression, pain, inflammation, appetite disorders, glaucoma and insomnia.
EP1966181A2 Anthranilic acid derivatives useful in treating infection with hepatitis c virus The present invention is directed to compounds of formula (I): wherein R1 is selected from the group consisting of -C(O)R and (a), wherein R6 and R7 are independently selected from H, alkyl, cycloalkyl, heterocycloalkyl, heteroaryl or aryl, any of which may be optionally substituted, G is selected from H or hydroxyl, Y is O, NH or S, X is selected from the group consisting of H, halo, alkyl, cycloalkyl, perfluoroalkyl, alkoxy, alkylthio, amino, alkylamino, dialkylamino, and CN, and n is 0, 1, 2 or 3, or a prodrug, a pharmaceutically acceptable salt, or a pharmaceutically active metabolite thereof. This invention is also directed to compositions containing compounds of the invention and methods of using both the inventive compounds and compositions thereof to treat or prevent Hepatitis C virus infection, or to inhibit replication of a Hepatitis C virus.
EP1651643A2 Bicyclic compounds and compositions as pdf inhibitors This invention is directed to novel bicyclic compounds, to the uses of these compounds in various medicinal applications, including treating disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections, and to pharmaceutical compositions comprising these compounds.
WO2014027112A1 Tris(hetero)arylpyrazoles and use thereof The present invention relates to novel tris(hetero)arylpyrazoles, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of retroviral disorders, in man and/or animals.
WO2009107262A1 Anticancer composition containing 3”-methylated epigallocatechin gallate It is intended to provide an anticancer composition which contains 3”-O-methylepigallocatechin gallate represented by the following formula (I).
CN101732296A Agomelatine-containing medicinal composition The invention provides an agomelatine-containing medicinal composition, which not only solves the problem of the dissolution of agomelatine in different crystal forms, but also meets the requirements of preparations for prescriptions and processes. The composition has the advantages of simple preparation process, convenience for operation, transport and storage, wide application range and suitability for large-scale production.
US20050032039 HIV-specific T-cell induction This invention discloses diagnostic, preventative, and treatment therapies of AIDS involving determining whether a subject exhibits an HLA-Cw7-restricted CTL response. Some methods are directed to the use of HLA-Cw7 as a genetic marker for long-term non-progression and amenability to treatment therapies. Diagnostic methods include a method for predicting long term non-progression in an HIV-infected subject. Preventative and treatment methods encompass determining whether a subject exhibits or can exhibit an HLA-Cw7-restricted CTL response. They also encompass ways of eliciting such a response, if necessary. Furthermore, some of the methods involve administering one or more HIV polypeptides or peptides, or polynucleotides encoding them, as a treatment therapy to prevent the development of AIDS.
CA2652516A1 Use of thymosin alpha 1 for preparing a medicament for the treatment of stage iv malignant melanoma It is described the use of thymosin alpha in combination with dacarbazine and optionally with Interferon alpha, for preparing a medicament for the treatment of malignant melanoma on stage IV characterized by distant unresectable metastases.
WO2007138114A1 Use of prodrugs for ocular intravireous administration This invention relates to the use of prodrug for the manufacture of a medicament useful for treating an ocular disease affecting the posterior segment of the eye, in a subject in need thereof, wherein the prodrug is a composition injected into the vitreous body, and the frequency of injections does not exceed one injection per month.
WO2005034935A1 Use of organoarsenic or organoantimony derivatives for their anticancer properties The invention relates to the use of at least one organoarsenic or organoantimony compound of formula (I) as defined in the description for producing a medicament for treating cancers and, in particular, leukemias, to the use of certain derivatives of formula (I) as a medicament as well as pharmaceutical formulations of derivatives of formula (I) in the form of nanovectors.
WO2012122969A1 Substituted diphenyl derivatives Triazene-substituted diphenyl derivatives are suitable as chemotherapeutic agents for treating carcinomas in humans and animals.
EP1335700B1 Pharmaceutical composition comprising chelating/sequestering agents and their dermatological use Pharmaceutical and cosmetical compositions comprising a chelating and a sequestering agent, and optionally containing further ingredients. Use of such compositions to make water more compatible with the skin. Use of such compositions to prevent or treat skin conditions such as eczema, irritation and skin dryness.
US20090023685 Nebulized or Sprayed Cidofovir for Recurrent Respiratory Papillomatosis A solution of 2.5-20% cidofovir is administered as droplets having a mean size of about 1 micron to about 20 microns either nebulized or as a spray to an individual having recurrent respiratory papillomatosis.
WO2006086992A3 Drug delivery systems containing phqspholipase a2 degradable lipid prodrug derivatives and the therapeutic uses thereof as. e.g. wound healing agents and peroxisome proliferator activated receptor ligands The present invention describes a lipid based prodrug and drug delivery system that can be used for treatment or alleviation of disorders that are associated with or resulting from increased levels of secretory phospholipase A2 (PLA2) in the diseased or injured tissue. In particular, the lipid based delivery systems are useful for administration of lipid prodrugs of lysophosphatidic acid (LPA) bioactive analogs, which are known to be potent biological mediators with e.g. growth stimulating and wound healing activities.
US20090088448 Rapamycin Derivatives and the Uses Thereof in the Treatment of Neurological Disorders Provided is a method of treating neurodegenerative disorders comprising administering to a subject in need thereof a compound of formula I:
US20110207726 Inhibitors of Human Cathepsin L, Cathepsin B, and Cathepsin S The present invention is directed to novel protease inhibitors that are specific for cathepsin L, cathepsin B, and cathepsin S. Accordingly, the present invention encompasses compositions and methods for treating and preventing diseases and disorders associated with cathepsin L, cathepsin B, or cathepsin S function or activity.
US20100086619 Dietary supplement containing strontium (M) ascorbate, compositions containing same, method for making same and method for using same A formulation including a compound of formula (ascorbate)2Sr:(M+a)x(ascorbate)y, or ascorbate)2Sr:Ca(ascorbate)2, together with calcium phosphate, vitamin D, D-Glucosamine, protein, fiber, flavoring agents, and optionally chondroitin is provided. A method for making the same together with a method of administering the same is also provided.
CN102617893A Preparation and application of composition of panaxoside Rg3, ginseng polysaccharide and ganoderan The invention discloses a preparation method of a medicinal composition containing ginseng polysaccharide, a high-Rg3-content panaxoside extract and ganoderan and an application of the medicinal composition for serving as an immune regulating agent. Measures such as enzymolysis, boiling water refluxing, alcohol extraction, ultrasonic treatment and the like are performed on an entire ginseng strain, so that a high-Rg3-content panaxoside extract and a ginseng polysaccharide extract can be obtained simultaneously. Measures such as smashing, enzymolysis, boiling water refluxing, ultrasonic treatment, alcohol extraction and the like are performed on lucid ganoderma, so that a ganoderan extract is obtained at high yield. On the basis, the obtained ginseng polysaccharide and ganoderan are mixed, foreign proteins and pigments are removed through one-step anion exchange chromatography, and a medicinal composition is obtained by combining panaxoside according to a certain proportion. The medicinal composition prepared with the method has the advantages of simple process, high immunoregulation activity and low cost.
EP1720554B1 Use of meloxicam for the treatment of respiratory diseases in pigs The invention relates to the use of meloxicam or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment or prevention of respiratory diseases in pigs.
WO2011118683A1 Patch for medical use Provided is a patch for medical use comprising a flexible pressure-sensitive adhesive layer which contains a large amount of a drug or a dissolution aid, yet is free from deformation and can be easily removed with little glue remainder. The patch for medical use comprises a drug having a secondary or tertiary amine structure in the molecule, a liquid auxiliary for the drug, and a resin composition wherein a copolymerized acrylic resin, which comprises a (meth)acrylate monomer as a main monomer component and has a functional group capable of reacting with an isocyanate group-containing cross-linking agent to thereby form a cross-linked structure, is cross-linked by the aforesaid isocyanate group-containing cross-linking agent that has been blocked.
US6841569 Treatment of central nervous system disorders; anticonvulsants, antiepileptics, neuroprotective agents and muscle relaxants Carbamate compounds of 2-heteroaryl-1,2-ethanediol are described. The compounds are effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.
US20110118287 Bicycloheteroaryl Compounds As P2X7 Modulators and Uses Thereof Bicycloheteroaryl compounds are disclosed that have formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
US20060293527 Analogs of epothilone Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell lines. Among the several bioactive analogs, the epothilone B analog with a thiomethyl thiazole ring stands out as the most potent.
CN1830444A Preparation method of Sophora flavescems injection An injection of kurarinol for treating chronic hepatitis and leukocytopenia is prepared from kurarinol through depositing in water, cold storage, ultrafiltration, further preparing in dark condition and N2 atmosphere, pouring in containers, sterilizing and lamp examining.
WO2007059871A1 Hydroxy-substituted diphenylazetidinones for the treatment of hyperlipidaemia The invention relates to compounds of the formula (I) in which R1, R2, R3, R4, R5 and R6 are defined as specified, and to their physiologically compatible salts. The compounds are suitable, for example, as hypolipidaemic drugs.
CN101284838A Ethylene imine derivates with thienopyridine, preparation method and applications thereof The invention belongs to the anti-platelet aggregation drug technical field and provides Piperazine derivatives containing thieno pyridine with the structure as showed in general formula (I) and pharmaceutically acceptable salt thereof, wherein R1 and R2=hydrogen, methyl, ethide, carboxyl and hydroxyl; R3=hydrogen; C1-C4 is for alkyl; C5-C6 is for naphthenic base; CH2R5, COR6, SO2R7, R8, R9 and R10 replace phenyl; R11 replace heterocyclic radical, wherein the definition of R4-R11 is the same as described in the instructions. The invention also relates to a preparation method of the compound, and meanwhile discloses a drug combination that uses the compound or the pharmaceutically acceptable salt as active ingredients and an application thereof in respect to anti-platelet aggregation drugs.
WO2009036753A2 Novel pharmaceuticals, method for the production thereof and use thereof in medical therapy The present invention relates to novel pharmaceuticals based on novel substituted 4-pyridine-3yl-pyrimidine, to a method for the production thereof, and to the use thereof in medical therapy, in particular cancer diseases.
US20080262099 Administering cannabidiol produced from a given cannabis chemovar and in the form of a botanical drug substance; modulators motility of glioma cell motility; uneffected by involvement of cannabinoid receptor antagonists; antitumor, anticarcinogenic, antiproliferative and antimetastsis agents. The invention relates to the use of a cannabis plant extract or a cannabinoid as a pharmaceutically active agent in the inhibition of tumour cell migration.
WO2007059356A3 Furfurylidene- pyrazolidines and their use as inhibitors of ubiquitin e1 The present invention features pyrazolidinyl compounds of formula (I) pharmaceutical compositions of substituted pyrazolidinyl compounds and methods of treating a patient suffering from cancer or viral infection, the method comprising administering to a patient one or more pyrazolidinyl compounds of the invention.
CN102440950A Doxycycline hydrochloride long-acting injection The invention discloses doxycycline hydrochloride long-acting injection and a preparation method thereof. The injection comprises the following components: 5-30% (W/V) of doxycycline hydrochloride, 25-70% (V/V) of compound organic solvent, 0.01-0.1% (W/V) of oxidation inhibitor, 0.5-10% (W/V) of magnesium compound complexing agent and 0.1-1% (W/V) of calcium compound complexing agent. The preparation method comprises the following steps of: mixing the components, adopting alkali to adjust the pH value to 8.0-9.0, and adding water for injection to 100% (V/V). According to the invention, the problem that doxycycline injection is easy to oxidize and decompose can be effectively solved.
WO2009063495A3 Substituted indole and its derivatives as cannabinoid modulators The present invention relates to novel substituted indole and indole derivatives to pharmaceutical compositions comprising the same, and to uses thereof. Compounds of the invention share pharmacological properties with cannabinoids and have a common wide range of beneficial therapeutic indications, hi particular, compounds of the invention are useful analgesic and anti-inflammatory agents by modulating the CB2 receptor.
WO2014083229A1 Use of metalloprotease inhibitors for the treatment of polycystic liver diseases The invention relates to the use of metalloprotease inhibitors for the treatment of polycystic liver diseases (PCLDs). The invention especially relates to the use of Marimastat as the preferred metalloprotease inhibitor for the treatment of PCLDs. Treatment with Marimastat can inhibit hepatic cystogenesis by blocking the metalloproteolytic hyperactivity of the polycystic cholangiocytes.
EP1423367B1 Solvates of lercanidipine hydrochloride and crystalline forms of lercanidipine hydrochloride The invention describes new solvates of lercanidipine hydrochloride with organic solvents, new crystalline Forms (III) and (IV) of lercanidipine hydrochloride obtained from said solvates by removing solvation solvents, and pharmaceutical compositions containing as active agent at least one of the crystalline Forms (III) and (IV) of lercanidipine hydrochloride.
CN101579350A Phosphatide composite, preparation method and application thereof The invention provides a phosphatide composite, a preparation method and an application thereof. The phosphatide composite is prepared by composing a total glycosides of paeony or a paeoniflorin or an albiflorin with the phosphatide, wherein the molar ratio of the phosphatide and the paeoniflorin is 0.5-2:1. The invention takes the phosphatide as a carrier to prepare the phosphatide composite, improves the solubility of the paeoniflorin, the total glycosides of paeony and the albiflorin, and improves the bioavailability, thus improving the drug effect. The method can prepare various preparations on pharmacy such as tablets, capsules, grains and the like, and can compose a drug combination together with other active components.
US20100291053 Inflammatory Disease Treatment We describe a composition comprising a source of long chain polyunsaturated fatty acid, for example, docosahexaenoic acid (DHA), and a carotenoid, for example, astaxanthin and other nutrients for prophylactic and/or therapeutic use in the healing of trauma- and stress-induced inflammatory conditions.
WO2011098607A1 Salts and hydrates of 4-[(3-chlor-4-fluoro-phenyl)amino]-6-(cis-4-{n-[(morph-1-olino-4-yl)carbonyl]-n-methyl-amino}-cyclohexane-1-yloxy)-7-methoxy-quinazoline, their use as drugs and their production The invention relates to a compound of formula (I), wherein x Q represents x H2O, x HCl or (x 0.5 HCl / x 1.5 H20), which have valuable pharmacological properties, especially an inhibitory effect on tyrosine kinase-mediated signal transduction, methods for the stereoselective production of this compound, especially of pharmaceutical formulations suitable to be inhaled and their use for the treatment of diseases, especially tumor diseases and benign prostatic hyperplasia, and of lung and respiratory diseases.
US20110142904 Methods for the In Situ Treatment of Bone Cancer The present invention relates to methods for in situ treatment of malignant cells from a cancer associated with bone. In one method, the treatment is for a primary cancer and entails positioning an implant containing and/or coated with at least one active agent for treating malignant cells directly in/on or indirectly among/near (e.g., by placing the implant in an area immediately proximal to) a site containing the malignant cells. In another method, the treatment includes positioning an implant containing and/or coated with at least one active agent for treating malignant cells directly in/on or indirectly among/near (e.g., by placing the implant in an area immediately proximal to) a surgical site from which malignant cells were previously removed/excised.
US20090264382 Methods for Treating Hematopoietic Neoplasms This invention relates to methods for treating, preventing and/or managing hematopoietic neoplasm in a subject by administering to the subject combretastatin A-4 phosphate, or a pharmaceutically acceptable salt thereof. The method may further comprise co-administering a chemotherapeutic agent.
CN101219195A Pharmaceutical composition, pharmaceutical formulation containing the composition and and uses thereof The invention relates to a drug combination and a drug preparation with the drug combination and the applications thereof, in particular to a drug combination for preventing and curing HIV infections. The invention comprises oil of zedoary turmeric and borneol, of which the weight ratio is 1: 0.2-2.2. The invention also provides the applications of the combination with oil of zedoary turmeric and borneol and the drug preparation thereof in preparing medicines for curing HIV infections.
CN102309474A Application of S-propargyl-cysteine to preparation of medicament for treating digestive system tumors The invention belongs to the field of pharmacy and relates to application of S-propargyl-cysteine (SPRC) to preparation of a medicament for treating digestive system tumors. In the invention, a class of broad-spectrum chemotherapeutic medicament, namely taxol, is adopted as a contrast, and in-vitro gastric cancer and liver cancer cell culture experiments are performed to detect the activities of caner cells. Results show that the SPRC in the invention can be used for decreasing cell survival rate, promoting cell apoptosis, decreasing cell proliferation and migration capabilities, enhancing apoptosis related factors Bax and p53, and reducing the mRNA (Messenger Ribonucleic Acid) and protein expressing level of an anti-apoptotic factor Bcl-2; and the SPRC is demonstrated to play a role in inhibiting the gastric cancer and the liver cancer. The SPRC can be prepared into treatment medicaments to be applied to treatment of the gastric cancer and the liver cancer.
US8394808 HM74 receptor agonists:xanthine derivatives, corresponding pharmaceutical compositions, treatment methods and processes The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
EP1110554B1 Medicinal compositions for treating eye diseases Medicinal compositions for treating eye diseases which contain as the active ingredient 2-alkynyladenosine derivatives having an acetylene bond at the 2-position of adenine base. Because of having a long-lasting and remarkable effect of lowering ocular tension, these compounds are useful as remedies for eye diseases with increased ocular tension or optic nerve failures such as glaucoma and hypertonia oculi.
WO2012055163A1 Letrozole type i crystal and preparation method thereof Disclosed is an anhydrous crystal of letrozole. The structure and characteristics of the anhydrous letrozole crystal are characterized by X-ray powder diffraction, differential scanning calorimetry, infrared spectrum and the like. The characteristic diffraction peaks of the crystal in a powder X-ray diffraction pattern at 2 θ are 13.08±0.2, 14.06±0.2, 17.04±0.2, 21.44±0.2 and 29.24±0.2 degrees. Also disclosed are a method for preparing the anhydrous letrozole crystal by using an anhydrous and pure organic solvent as a crystallization solvent, and using the crystal in a pharmaceutical formulation for antiestrogen therapy for treating menopausal patients with advanced breast cancer.
US20060074044 Nucleotide sequences coding stem cell factors for use as therapeutic tools in treating learning and memory disorders The invention provides novel polynucleotides and polypeptides encoded by such polynucleotides and mutants or variants thereof the correspond to a novel human secreted stem cell growth factor-like polypeptide. These polypeptides comprise nucleic acid sequences isolated from cDNA libraries prepared from human fetal liver spleen, ovary, adult brain, lung tumor, spinal cord, cervix, ovary, endothelial cells, umbilical cord, lymphocyte, lung fibroblast, fetal brain, and testis. Other aspects of the invertion include vectors containing processes for producing novel human secreted stem cell growth factor-like polypeptides, and antibodies specific for such polypeptides.
CN101703484B Preparation method of hexadecadrol sodium phosphate freeze-dried powder injection The invention provides a preparation method of hexadecadrol sodium phosphate freeze-dried powder injection, which comprises the following steps: mannitol is dissolved, added with active carbon, boiled and filtered, added with the hexadecadrol sodium phosphate and prepared to a liquid medicine; the liquid medicine is treated by prefreezing, primary freeze drying and secondary freeze drying; and then hydraulic pressure adding stopper, rolling cap and packaging are carried out. The method has the advantages that the method improves the liquid medicine preparation and freeze-drying technology, does not affect the content of the hexadecadrol sodium phosphate, can increase the single batch output, simultaneously shortens the freeze-drying time, increases the product stability, saves the energy,increases the production and reduces the production cost.
US20100092573 Hemostatic bio-material composition and method The present invention relates to a haemostatic bio-material composition and method for achieving hemostasis. The method for providing hemostasis generally comprises: supplying a dry potassium phosphate based hemostat mixture comprising: monobasic potassium phosphate, a metal oxide, and a tertiary calcium phosphate, wherein the weight percent ratio of monobasic potassium phosphate to metal oxide is between about 3:1 and 1:1; mixing the dry potassium phosphate based hemostat mixture with an aqueous solution forming an activated hemostat slurry; applying an hemostasis-promoting amount of the activated potassium phosphate based hemostat slurry to a site of bleeding; wherein the site of bleeding is in, on, or proximate to bone.
CN1927384A Lung lobe cleaning fluid The invention relates to lung lobes cleaning solution which is a kind of lithicosis cleaning substance. The content for every ingredient of the solution goes as follows: Na+134-145mmol/L,K+3.5-4.5mmol/L, Cl-90-110mmol/L, PO4-348.5-65.6mmol/L, dextran 10-20g/L, antigut 1-5mmol/L, glutathion 1-3mmol/L, calparine 500-1000U/L, decaesadril 5-10mg/L, verapamil 10-20mg/L, 1.0-5.0g/L ampicillin, penicillin 800-8000 thousand U, the final pH of the solution is 7.0-7.5. The cleaning solution can not only remove the dust and foreign substances, it can also improve the microcirculation of lung lobes and relieve the reaction after cleaning so as to avoid the impact of cleaning to the lung functions and can be applied in the treatment and second-level prevention of lithicosis.
CN102482264A 2-carboxamide-7-piperazinyl-benzofuran derivatives 774 The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1- 4alkylheterocyclyl, heterocyclylheteroaryl, arylheterocyclyl, carbocyclylheteroaryl, heterocyclylaryl, optionally substituted R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted R4 is hydrogen, halogen, methyl or methoxy to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.
WO2011057269A2 Compositions for enhancing hair growth Methods and compositions for stimulating the growth of hair are disclosed wherein emulsions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R1 and R2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal.
WO2006088017A1 Sugar chain containing 4-position halogenated galactose and application thereof An oligosaccharide having at an end thereof a 4-position halogenated galactose residue represented by the following formula (I); a transferase inhibitor containing the oligosaccharide; a method of inhibiting a sugar chain elongation reaction by glycosyltransferase with the use of the inhibitor; etc. Further, there is provided a process for producing a 4-position halogenated galactose sugar nucleotide represented by the formula (II) with the use of microbe-derived galactokinase and microbe-derived hexose-1-phosphate uridyl transferase. (I) (wherein X is a halogen atom; and R is a monosaccharide, an oligosaccharide or a carrier) (II) (wherein each of R1 to R3 is hydroxyl, acetyl, a halogen atom or a hydrogen atom; X is a halogen atom; and M is a hydrogen ion or a metal ion). Thus, there are provided a sugar chain containing 4-position halogenated galactose whose use in pharmaceutical products, etc. is promising, and applications thereof.
CN101249086A Use of peroxyacetic acid in fish cultivating The invention discloses the use of peracetic acid in fish culture. The invention proposes that peracetic acid is used as a drug for treating and preventing fungal diseases in cultured fish, including saprolegniasis, branchiomycosis, mucormycosis and fusaridiosis; and also used for fungal infections of fish during transportation. Further, peracetic acid is used for disinfection of hatching equipment and pretreatment of water during hatching of fish eggs, thereby reducing the incidence of fungal infections of fish eggs during hatching of fish eggs. Compared with the existing drugs for controlling fungal diseases in fish, peracetic acid has the advantages of strong antifungal activity, no residue and no pollution. Additionally, peracetic acid also has bactericidal and parasiticidal effects and can increase oxygen content in water body.
US8648082 Gum resin as a carrier for topical application of antimicrobial agents The invention provides a biological dressing for treatment of a dermatological disease comprised of a gum resin, a topically acceptable volatile solvent, and a pharmacologically active agent. The gum resin is present in a suitable amount that the composition, when the solvent evaporates, will dry to form a solid coating that sticks to the skin or mucosal membrane to which the composition is applied and maintain the pharmacologically active agent over a sustained period of time in contact with sites on the skin or mucosal membranes exhibiting symptoms of the disease. Methods are provided for treating symptoms of dermatological diseases with such a pharmacological composition. Biological dressings including tincture of benzoin and clotrimazole are shown to be efficacious for the long-term amelioration of symptoms of athlete's foot.
US20080146602 3-Chloro-2-[(2,4-dioxo-1,3-oxazolidin-3-yl)methyl]-5,6,7,8-tetrahydro-4-(4-methoxyphenyl)[1]benzothieno[2,3-b]pyridine-7-carboxamide, salts and prodrugs, used as antiinflammatory agents and for treatment of autoimmune diseases A compound represented by the formula (I) wherein R is a hydrogen atom or a C1-4 alkyl group, and X is CH2, O or S, or a salt thereof. The present invention provides a novel thienopyridine derivative having an anti-inflammatory effect, a bone resorption suppressing effect, an immune cytokine production suppressing effect and the like, and useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of arthritis such as rheumatoid arthritis and the like, and the like, and the like.
EP1077994B1 Imidazolidine derivatives, the production thereof, their use and pharmaceutical preparations containing the same The invention relates to imidazolidine derivatives of formula (I), in which B, E, W, Y, R, R?2, R3, R30¿, e and h have the meanings cited in the claims. The compounds of formula (I) are valuable medicament active agents which are suited, for example, for treating and preventing inflammatory diseases, for example, rheumatoid arthritis, or allergic disorders. The compounds of formula (I) are inhibitors of adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4 which belong to the group of integrins. They are generally suited for treating or preventing diseases which are caused by an undesirable degree of leukocyte adhesion and/or leukocyte migration or are connected therewith or with which cell-cell interactions or cell-matrix interactions play a roll. Said interactions are based on interactions of VLA-4 receptors with the ligands thereof. The invention also relates to a method for producing the compounds of formula (I), to the use thereof, especially as medicament active agents, and to pharmaceutical preparations which contain compounds of formula (I).
EP1030667B1 Use of mirtazapine for the manufacture of a medicament for treating sleep apneas The compound mirtazapine is found to be effective in treating sleep apneas. Optionally, mirtazapine is combined with an SSRI such as fluoxetin.
US7723503 nucleotide sequences or complements that encode polypeptides having omega-3 desaturase and delta-12 desaturase enzyme activity, used for making polyunsaturated fatty acids; additives for drugs, nutritional compositions, animal feeds, as well as other products such as cosmetics Disclosed are isolated polynucleotides encoding an omega-3 desaturase and a delta-12 desaturase, the enzymes encoded by the isolated polynucleotides, vectors containing the isolated polynucleotides, transgenic hosts that contain the isolated polynucleotides that express the enzymes encoded thereby, methods for producing the desaturase enzymes, and method of using the enzymes to make polyunsaturated fatty acids. The isolated polynucleotides are derived from a fungus, Saprolegnia diclina (ATCC 56851). In particular, omega-3-desaturase may be utilized, for example, in the conversion of arachidonic acid (AA) to eicosapentaenoic acid (EPA). Delta-12 desaturase may be used, for example, in the conversion of oleic acid (OA) to linoleic (LA). EPA or polyunsaturated fatty acids produced therefrom may be added to pharmaceutical compositions, nutritional compositions, animal feeds, as well as other products such as cosmetics.
US6951857 Interleukins; cytokines; for treating eosinophil-dependent inflammatory disease/bronchial asthma The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R1 represents hydrogen, C1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, mercapto, C1-6alkylthio, C3-7cycloalkyl, aryl or C1-6alkyl substituted with mono- or di(C1-6alkyl)amino, C1-6alkyloxy, aryl or Het; R2 represents cyano or a radical of formula —C(═X)—Y—R5; wherein X represents O or S; Y represents O, S, NR6 or a direct bond; R5 represents hydrogen; C3-7cycloalkyl; aryl or optionally substituted C1-6alkyl; and where Y is a direct bond, R5 may also be halo or Het; R3 and R4 each independently represents halo, haloC1-6alkyl, C1-6alkyl, hydroxy, C1-6alkyloxy, C1-6alkylcarbonyloxy, mercapto, C1-6alkylthio, C1-6alkylsulfonyl, C1-6alkylsulfinyl, haloC1-6alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C1-6alkyl)amino or (C1-6alkylcarbonyl)amino; aryl represents phenyl or substituted phenyl; and Het represents an optionally substituted heterocycle; in the manufacture of a medicament useful for treating eosinophil-dependent inflammatory diseases. The invention also relates to novel compounds, their preparation and compositions comprising them.
US20090317395 Antimicrobial Peptide Derived from Galanin Message Associated Peptide (GMAP) The present invention relates to a new antimicrobial peptide, comprising the amino acid sequence of human galanin message associated peptide (GMAP) or a homolog, ortholog, chemically modified variant or antimicrobially active variant thereof, and respective uses thereof, particular in the topical treatment of antimicrobial diseases.
US20060110465 Compositions addressing inflammation and/or degenerative disorders Compositions for primarily addressing degenerative complaints, in particular joint related conditions such as arthritis and rheumatism, in which there may also be associated inflammation, are provided. Other potential uses are also discussed, as well as prophylactic and curative applications. Preferred embodiments incorporate green-lip mussel products (particularly GLME) with shark cartilage or chondroitin compounds, and plant and bark based antioxidants are employed in a number of embodiments.
CN103467492A Aspoxicillin compound, pharmaceutical composition, preparation and preparation method thereof The invention belongs to the field of pharmacy, concretely relates to Aspoxicillin compound, pharmaceutical composition, preparation and preparation method thereof. The X-ray powder diffraction pattern of Aspoxicillin compound measured by Cu-Kalpha ray is shown in the figure 1. The dosage forms of the pharmaceutical composition comprise freeze-drying powder injection, aseptic powder injection and injection, and freeze-drying powder injection is preferable. Stability test confirm that pharmaceutical composition and preparation prepared from Aspoxicillin compound have good stability, and are suitable for clinic application.
CN102784144A Compound clotrimazole combination for treating livestock dermatomycosis and preparation method thereof The invention relates to a compound clotrimazole combination for treating livestock dermatomycosis and a preparation method thereof. The combination is prepared by uniformly mixing the following components in parts by weight: 3-5 parts of clotrimazole, 2-4 parts of ketoconazole, 1-3 parts of lauryl sodium sulfate, 3-5 parts of octadecanoic acid, 3-5 parts of white vaseline, 24-28 parts of liquid paraffin, 2-4 parts of castor oil, 0.4 parts of ethylparaben, 1-3 parts of PEG-400 (polyethylene glycol-400), 1-3 parts of essence, 40-60 parts of distilled water and the like. The compound clotrimazole combination has the beneficial effects of reasonable formulation, simplicity in preparation, quite obvious curative effect and special livestock dermatomycosis treatment effect proven by clinical application.
WO2007033578A1 Metallo-fullerenols and its application in preparation of medicines for inhibiting the growth of tumour A metallo-fullerenols of general formula M@C2m(OH)x and a tumor- inhibiting composition comprising the metallo-fullerenols are new, wherein M in general formula M@C2m(OH)x is selected from the rare-earth matal of La or Gd, m=41or 30 and 10≤x<50. The metallo-fullerenols of general formula M@C2m(OH)x also is used to prepare the medicine for inhibiting the growth of tumour.
CN102250099A Non-peptide thrombin inhibitors as well as preparation method and medical application thereof The invention relates to the field of pharmaceutical chemistry, and particularly relates to non-peptide thrombin inhibitors (I), as well as a preparation method and an inhibition effect thereof on thrombin. The formula I is shown in the specification, and n and R are defined in the specification. Pharmaceutical experiments prove that the compounds (I) provided by the invention have stronger inhibition effect on thrombin.
EP1496883A1 Method for treating ileus with an alpha-ketoalkanoic acid, ester or amide Disclosed is a method for treating ileus in a subject. The method comprises the step of administering to the subject an effective amount of an alpha-ketoalkanoic acid, a physiologically-acceptable salt of an alpha-ketoalkanoic acid, an ester of an alpha-ketoalkanoic acid, or an amide of an alpha-ketoalkanoic acid.
CN102657672A Veterinary compound tulathromycin nanoemulsion and preparation method thereof The invention discloses veterinary compound tulathromycin nanoemulsion injection. Particle size of the nanoemulsion ranges from 1nm to 100nm and is made of the following raw materials in percentage by weight: 30%-40% of surfactant, 5%-15% of cosurfactant, 5%-15% of oil, 2%-5% of tulathromycin, 0.5%-1.25% of trimethoprim lactate, and the balance of deionized water. Bacteriostasis is achieved by administration of the injection once, and the bacteriostasis is quick and is slowly released. The nanoemulsion is capable of avoiding first pass effect of hepar and has neural pH so that animal stress reaction is reduced. The veterinary compound tulathromycin nanoemulsion injection is high in safety, simple to prepare and low in energy consumption, can be produced massively without special equipment, and has broad market prospect in the field of medicine.
US7122208 Administering aliquot of blood which has been treated ex vivo with stressors such as oxidation, thermal stress and electromagnetic radiation; wherein concentration of reactive oxygen species in neuronal cells or tissues is reduced Disclosed are methods for treating and preventing neurological disorders which have a significant inflammatory component. The methods of the present invention involve extracting blood from a patient, subjecting the blood ex vivo to at least one stressor selected from the group consisting of an oxidative environment, thermal stress and UV light, and then re-administering the blood to the patient, thereby reducing inflammation.
CN101074255A Preparation of hemsleyadine-A and its use of preparing pharmaceutics against cancers Production of medicinal component snow bile pigment and its usage for preparing medicines in treatment of cancers are disclosed. The process is carried out by taking snow bile plant tuber, crushing, taking acetone 18-26 proportion as solvent, extracting by diacolation method, recovering extract in water-bath kettle at 60-75 degree to obtain extractive, adding extractive into silica gel 1-2 proportion, drying to obtain silica-gel column, gradient eluting by ethanol or chloroform with volume concentration 2-10%, recovering eluent to obtain coarse product, heating while dissolving for ethanol or alcohol in water bath, filtering, lowering to room temperature, re-crystallizing to obtain prism crystal with purity above 98%. It can be used to prepare medicines in treatment of hepatocarcinoma, lung cancer, gastric carcinoma, laryngeal cancer and leukemia.
US7056525 Use thereof in human and animal foods, cosmetics and pharmaceuticals; soft gelatin capsules Carotenoid formulations comprising a mixture of β-carotene, lycopene and lutein, and the use thereof in human and animal foods, cosmetics and pharmaceuticals.
CN103536535A Dabigatran etexilate liposome The invention provides dabigatran etexilate liposome. The dabigatran etexilate liposome is characterized by consisting of at least one phospholipid and a lipophilic compound. The dabigatran etexilate liposome preferably comprises the following components in parts by weight: 1 part of dabigatran etexilate, 10 to 50 parts of lecithin and 1 to 10 parts of cholesterol. The invention also provides a dabigatran etexilate liposome solid preparation. The dabigatran etexilate liposome solid preparation is prepared from the following components in parts by weight: 1 part of dabigatran etexilate liposome, 1 to 3 parts of a filling agent, 0 to 0.2 part of a disintegrating agent, 0.02 to 0.1 part of an adhesive and 0 to 0.08 part of a lubricating agent. The solid preparation can also comprise 0 to 10 parts of a corrigent and 0 to 0.15 part of a flavoring agent. According to the technical scheme of the invention and the advantages of the liposome, the medicine adsorption and utilization ratio of dabigatran etexilate is increased, the half-life period of the medicine is prolonged, and the administration dosage or the administration frequency can be effectively reduced.
CN1789263A Substituted piperazidine-piperidine amide compound, preparation method and uses thereof The invention discloses a groups of substituted piperazine-piperidine acidamide compounds, process for preparation and use, wherein aryl formaldehyde is used as the raw material, and is subject to reduced ammoniation reaction with Grignard reagent, finally amidation reaction is employed to obtain the compounds of general formula (I).
US20110160173 Method Of Treating Human Skin And A Skin Care Composition For Use In Such A Method One aspect of the invention concerns a cosmetic method of treating human skin by delivering an estrogenic component to said skin. The method comprises applying to the skin a composition containing: (i) at least 5 μg/g of an estrogenic component selected from the group consisting of substances represented by the following formula (I) in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors; and (ii) a cosmetically acceptable vehicle. Other aspects of the invention relate to therapeutic methods of treating or preventing vaginal dryness or acne and a therapeutic method of promoting wound healing. Yet another aspect of the invention relates to a skin care composition comprising the aforementioned estrogenic component and a cosmetically acceptable vehicle.
CN101167740B Compound sodium acetate electrolyte injection and preparation method thereof The utility model relates to the technical field of chemical, in particular to a compound electrolyte injection of sodium acetate and process for preparation, wherein the compound electrolyte injection of sodium acetate takes natrium chloride, potassium chloride, calcium gluconate, magnesium chloride, sodium acetate, sodium citrate and glucose as raw materials. The compound electrolyte injection of sodium acetate of the invention is called sodium acetate equilibrium liquid because pH, osmotic pressure and molar concentration containing various particles are approximate to extra cellular fluidof human body. The invention is used to treat shock caused by oligemia of circulating blood and reduction of tissue fluid caused by operation, trauma, scald and profuse bleeding, to replenish and adjust the extra cellular fluid, to correct metabolic acidosis and to substitute partial blood transfusion as a crystalloid blood volume extended dose. The invention has the advantages of doing effectively organ perfusion, maintaining circularity stable, replenishing electrolyte, improving hyponatremia during shock, preventing and correcting acidosis.
CN1813920A Medicinal composition with synergistic effect The present invention relates to a medicinal or functional health-care product composition, its preparation method and application. The composition contains natural plant extract or monomer active component. Said medicine composition can be used for preventing and curing the diseases of diabetes and its complicating disease, senile dementia, angiocardiopathy, cerebrovascular disease, hyperlipemia, fatty liver and others.
CN101230083A Novel glycyrrhetinic acid derivatives and preparation method thereof The invention provides compound provided with the structure as shown in formula I and the hydrate thereof. The compound can be used as ant-ulcer medicine; wherein, M1 and M2 are metallic ions, which includes sodium, potassium, zinc, magnesium, bismith, and aluminum, M1 and M2 can be identical and can also be different, and the quantity of the metallic ions are correlated with the valency thereof.
US20120046330 Pharmaceutical compositions of (r)-1-(2,2-difluorobenzo[d] [1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration thereof A pharmaceutical composition comprising Compound 1, (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.
CN101129348A Use of dipropylacetic acid or its salt in treating tumour The invention relates to the medicinal use of dipropylacetic acid in the treatment of gastric carcinoma, lung carcinoma, hepatic carcinoma, breast cancer, colon cancer, cancer of pancreas, intestinal cancer, esophagus cancer, cervical carcinoma, bladder carcinoma, renal carcinoma, sarcoma or melanin cancer.
US20100098750 Pharmaceutical composition comprising phenylamidine derivative and method of using the pharmaceutical composition in combination with antifungal agent A pharmaceutical composition comprising a phenylamidine derivative or a salt thereof, represented by a general formula, wherein R1 and R2 may be same or different, and represent an optionally substituted C3-4alkyl group; and one or more agents selected from azole antifungal agents, polyene antifungal agents, candin antifungal agents and fluoropyrimidine antifungal agents, and a method for combination use of the phenylamidine derivative or a salt thereof and the agents are useful for treating fungal infections caused by a fungal pathogen.
US20070281974 1 h-imidazole derivatives as cannabinoid receptor modulators The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders in which cannabinoid receptors are involved. The compounds have the general formula (I) wherein R, R1—R4 and X have the meanings given in the specification.
WO2008076269A3 MONOPHOSPHATES AS MUTUAL PRODRUGS OF MUSCARINIC RECEPTOR ANTAGONISTS AND β-AGONISTS FOR THE TREATMENT OF COPD AND CHRONIC BRONCHITIS A mutual prodrug of a MRA and a β-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 μL) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5 μ, produced by nebulization or by dry powder inhaler.
EP1100878B8 Process for producing genetically modified cd34-negative adherently growing haematopoietic stem cells The invention relates to the use of genetically modified, very early haematopoietic and mesenchymal stem cells (negative for the expression of the surface molecule CD34) in the individual gene therapy of mono- or oligogenetic diseases or in cell therapy. Autologous CD34-negative adherently growing stem cell cultures from the peripheral blood of the patient are applied and efficiently transfected or infected with genetic constructs. The gene products of these genes should substitute defective or absent proteins or factors in the patient organism in the long term. After expansion, the autologous stem cells can also be used for cell therapy (organ replacement therapy).
CN1718185A Long-acting anethol trithione prepn. and its prepn. method A long-acting anethol trithione is proportionally prepared from anethol trithione and conventional slow-releasing auxiliary. Its preparing process is also disclosed.
WO2014096697A1 Use of acetylsalicylic acid to prevent and/or treat diabetic wounds The present invention relates to acetylsalicylic acid or a salt thereof, at a concentration comprised between 200 and 4800 μΜ, for use in the prevention and/or treatment of diabetic wounds.
CN102451249A Drug for treating burn and scald, and application thereof The present invention provides a drug for treating burn and scald. The drug comprises a drug composition and/or a pharmaceutically-acceptable carrier, and is characterized in that: the drug composition mainly comprises the following raw material drugs, wherein the raw material drugs comprise, by weight, 10-20 parts of common melastoma herb, 15-25 parts of narrowleaf screwtree root, 10-25 parts of mallotus apelta, 10-20 parts of breynia fruticosa, 10-20 parts of parasite scurrula, 10-20 parts of rhapniolepisindica, and a proper amount of antibiotic. The application for the drug comprises that: according to the weight part ratio, the raw material drugs are dried in the sun and grinded, a debridement treatment is performed on a wound, then the wound is cleaned, the blister is pierced from the side surface by using a sterile needle to remove the water, the blister skin removal is not required, the grinded raw material drugs are externally coated on the wound position, and the dressing is not required, such that the disease condition is easily observed, and the pain on the patient during the dressing changing process is reduced. The drug is usually applied twice a day, and the effect can be provided after continuously using the drug for about a week.
EP1694316A1 Memantine for the prevention or reduction of suicidality and for treatment of major depression associated with suicidality The present invention relates to the treatment of major depressive disorder (MDD), and the prevention of suicidality associated therewith, using the uncompetitive NMDA receptor antagonist memantine.
WO2005077948A1 Fungicidal heterocyclic compounds The invention provides compounds which exert fungicidal activities based on the mechanism of action of the inhibition of 1,6-β-glucan synthesis with broad spectra specifically or selectively; and fungicides containing the compounds, salts thereof, or solvates of both. Compounds represented by the general formula (I), salts thereof, or solvates of both.
CN1957938B Effervescence tablet of Glucurolactone, and preparation method An effervescent tablet of glucuronolactone for protecting liver contains glucuronolactone, pharmacologically acceptable acid-base pairs, additive, adhesive, lubricant, sweetening agent and flavouring. Its preparing process is also disclosed.
CA2593793A1 Compounds and methods for regulating triglyceride levels The present invention provides use of vitamin B6 related compounds for the treatment and prevention of hypertriglyceridemia.
CN102018680A Emedastine difumarate sustained release tablets and preparation method thereof The invention discloses emedastine difumarate sustained release tablets, which are prepared from the following raw materials by weight: 2mg of emedastine difumarate, 40mg of carbopol resin, 75mg of povidone K30 and 50mg of cyclodextrine. The preparation method comprises the following steps of: a, mixing the emedastine difumarate and the carbopol resin according to an equivalent incrementing method; b, mixing the mixture and the povidone K30, adding ethanol and stirring for dissolution; c, adding the cyclodextrine to prepare a soft material, preparing granules with the granularity of 20 meshes, and drying at the temperature of between 50 and 70 DEG C; d, processing the granules; and e, tabletting. By taking the carbopol resin, the povidone K30 and the cyclodextrine as framework materials and by adopting the wet-process pelletizing and tabletting technology, the emedastine difumarate sustained release tablets are smooth in surfaces, good in hardness and high in release stability and do not fall off in the coating process.
CN101862374A Lotus plumule and new application of extractive thereof The invention provides a new application of lotus plumule, in particular to the application of the lotus plumule, lotus plumule total alkaloid, bisbenzylisoquinoline-(7-0-11')-monoether key alkaloid derivant or analogue in preparing a drug or health care food of 5 alpha-reductase inhibitor. The invention also provides a 5 alpha-reductase inhibitor. The lotus plumule of the invention serves as the 5 alpha-reductase inhibitor and can serve as drug, health care food or food additive. The lotus plumule and the active ingredients thereof of the invention are used for inhibiting 5 alpha-reductase, can reduce prostate gland, can quickly remove the obstruction symptom of benign prostatic hyperplasia, can treat seborrheic alopecia and acne, has specific potency and controllable quality, is safe and provides a new option for clinic.
EP0910428B1 Photopheresis treatment of chronic hcv infections A method of treating chronic HCV infections is disclosed. The method involves the optional treatment of a patient with interferon alpha and the treatment of a patient's blood with a psoralen compound followed by ultra violet light-activation of the psoralen compound. The blood treated as such is returned to the patient in a process known as extracorporeal photopheresis.
US20060122218 e.g. (2R,3S)-2-(2,3-Dichlorophenoxymethyl)-8-methyl-3-(2-thienyl-8-aza-bicyclo[3.2.1]octane; antidepressants; anxiolytic agents This invention relates to novel 8-aza-bicyclop[3.2.1]octane derivatives useful as monoamine neurotransmitter re-up-take inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
CN102058555A Doxazosin controlled release tablet The invention relates to a doxazosin controlled release tablet composition which contains effective quantities of doxazosin and polyoxyethylene and selectively comprises one or more pharmaceutically acceptable auxiliary materials. The invention also relates to a doxazosin controlled release tablet which comprises a single layer of tablet core and a coating film wrapped on the tablet core, medicine release holes are arranged at one side of the tablet, the tablet core comprises effective quantities of doxazosin and polyoxyethylene and selectively comprises one or more pharmaceutically acceptable auxiliary materials, and the coating film is a semi-transparent film.
US7109339 Substituted tricyclic gamma-carbolines as serotonin receptor agonists and antagonists The present invention is directed to novel compounds represented by structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R4a, R5, R6, R7, R8, R9,and m, are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain central nervous system disorders. The compounds of this invention are serotonin receptor modulators, in particular 5HT2C receptor agonists and antagonists, and are useful in the control or prevention of central nervous system disorders including obesity, anorexia, bulemia, depression, anxiety, psychosis, schizophrenia, migraine, addictive behavior, obsessive-compulsive disorder, and sexual disorders.
EP1263763B1 Tubulin binding ligands A diverse set of tubulin binding ligands have been discovered which are structural by characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, and phosphoramides capable of demonstrating selective targeting and destruction of tumor cell vasculature.
US20100322862 Methods and compositions using peptides and proteins with c-terminal elements Disclosed are compositions and methods useful for targeting and internalizing molecules into cells of interest and for penetration by molecules of tissues of interest. The compositions and methods are based on peptide sequences that are selectively internalized by a cell, penetrate tissue, or both. The disclosed internalization and tissue penetration is useful for delivering therapeutic and detectable agents to cells and tissues of interest.
US20100305205 Composition and/or method for preventing recurrence of stroke By using a composition for preventing onset and/or recurrence of stroke which contains ethyl icosapentate as its effective component, onset and/or recurrence of stroke is prevented, or in particular, the onset and/or recurrence of stroke in a hyperlipidemia patient who has been treated with HMG-CoA RI, or in particular the recurrence of stroke in a patient who is beyond six months after the onset of stroke, is prevented.
US20080280891 effective against a broad range of cancers, especially leukemia, non-small cell lung and colon; (6-chloropyridin-3-yl)-[3-hydroxy-5-(1H-indol-4-yl)-phenyl]-methanone; antimitotic agents that can block cell cycle progression The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.
US8106042 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives useful as modulator of nicotinic acetylcholine receptors This invention relates to novel N-oxides of a 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivative and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
WO2011074519A1 Pharmaceutical composition for treatment and prevention of age-related memory impair Disclosed are: a pharmaceutical composition for treating and preventing age-related memory impair; and others. Specifically disclosed is a pharmaceutical composition for treating and/or preventing age-related memory impair, which is characterized by containing lactic acid and/or a derivative thereof.
EP2643324A1 Antifungal 5,6-dihydro-4h-pyrrolo[1,2-a][1,4]-benzodiazepines and 6h-pyrrolo[1,2-a][1,4]benzodiazepines substituted with phenyl derivatives The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines of Formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
CN1651423A Felt wort extract, its preparation method and use An extract of a Chinese-emdicinal herb 'Maohouqiaoruihua' used to prepare medicine for preventing and treating asthma and bronchitis is prepared through crushing the raw material, extracting in alcohol solution, and purifying by macroreticular resin.
CN1853639A Medical use of surface active substance An application of the surfactant (cholalic acid, tween-80, etc) in preparing the medicines to prevent and/or treat the acute pulmonary injury-acute respiratory distress syndrome, such as pulmonary edema, is disclosed.
EP1148881B1 USE OF PYRIDAZINO ¬4,5-(b)|-INDOLE-1-ACETAMIDE DERIVATIVES FOR PREPARING MEDICINES FOR TREATING DISEASES RELATED TO THE DYSFUNCTION OF PERIPHERAL BENZODIAZEPIN RECEPTORS The invention concerns the use of a compound of general formula (I) wherein: X represents a halogen atom; Y represents one or several atoms or groups selected among hydrogen, halogens and hydroxy, methyl, methoxy and nitro groups; R1 represents a C1-C4 alkyl group; R2 and R3 represent each a hydrogen atom or a C1-C4 alkyl group, or R2 and R3 together form with the nitrogen atom bearing them, a pyrrolidinyl, piperidinyl or morpholinyl group, for preparing a medicine for preventing or treating diseases and disorders related to the peripheral benzodiazepin receptor.
CN101284004A Application of two bi-sesquiterpenes compound for preparing antineoplastic and antiinflammatory medicine The invention relates to an application of two sesquiterpenoids in preparing antitumor and anti-inflammatory medicines. The sesquiterpenoids are gochnatiolide A and gochnatiolide B, which can be extracted and separated from Ainsliaea fulvioides or other plants, or obtained by chemical synthesis. The experimental results show that the two sesquiterpenoids have good inhibitory effect on human tumor cells and have distinct inhibitory effect on inflammations. Therefore, the two sesquiterpenoids can be used for preparing antitumor and anti-inflammatory medicines.
WO2006090206A1 Improved extracts of psidium guajava l., methods for its obtaining and use for the treatment of gastrointestinal disorders The invention is related to the obtaining of phytomedicaments that contain standardized extracts coming from the guava plant (Psidium guajava L.), particularly from its leaves (Psidii guajavae folium), useful for the treatment of diverse gastrointestinal diseases related to dysfunctions of the nervous system associated to gastrointestinal function. The anti-microbial, anti-motility, anti-spasmolytic, anti-inflammatory, anti-oxidant and anti-secretor properties of the clinically evaluated phytomedicaments of the invention, as well as its null toxicity, allow its usage in the clinic for the treatment of disorders of the gastrointestinal function.
US20090130194 Methods of Treating Cancer with High Potency Lipid-Based Platinum Compound Formulations Administered Intravenously In one aspect, the present invention relates to methods of treating cancer in a patient comprising administering intravenously to a patient in need thereof a cancer treating effective amount of a lipid-complexed platinum compound composition wherein the concentration of the platinum compound of the lipid-complexed platinum compound composition is greater than about 1.2 mg/ml.
CA2420026C 1alpha-hydroxy-2-methylene-19-nor-homopregnacalciferol and its therapeutic applications This invention discloses 1.alpha.-hydroxy-2-methylene-19-nor-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte this evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any calcemic activity and therefore may be used to treat immune disorders in humans as well as renal osteodystrophy.
CN103044453A Cefamandole nafate compound and pharmaceutical composition thereof The invention relates to a cefamandole nafate compound and a pharmaceutical composition of the cefamandole nafate compound. The cefamandole nafate compound is crystal, and is determined by X-ray powder diffraction, and the characteristic peak in an atlas is shown as 8.8 degrees, 9.5 degrees, 10.2 degrees, 11.3 degrees, 12.0 degrees, 14.4 degrees, 16.8 degrees, 17.3 degrees, 20.6 degrees, 25.0 degrees, 27.8 degrees, 28.1 degrees and 30.2 degrees in a range of 20+/0.2 degrees. The pharmaceutical composition of the cefamandole nafate compound is a preparation and a pharmaceutical composition preparation containing the above cefamandole nafate compound and the preparation is powder-injection. The cefamandole nafate crystalline compound is high in stability and few in insoluble particles; a cosolvent is not needed, so that the compound can be directly and aseptically sub-packaged to obtain cefamandole nafate powder injection for injection. The cefamandole nafate crystalline compound is also fully mixed with aseptic sodium carbonate powder to be aseptically sub-packaged. The number of insoluble particles added with the powder injection of sodium carbonate is few on the basis of reaching standard request.
WO2012000087A1 Compositions and methods for controlling blood glucose levels Disclosed herein are methods and compositions for controlling the blood glucose levels of a patient with diabetes, comprising administering a composition comprising an effective amount of Gudmar, Kalijiri, Kariyatu,Neempan, Methi, Mamejava, and Karela.
WO2014055588A1 Treatment of mild and moderate alzheimer's disease The present invention relates to methods of treatment using [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl amine ("COMPOUND I") or a pharmaceutically acceptable salt thereof. In various embodiments, the methods of treatment include treatment of mild-to-moderate dementia of Alzheimer's type, diabetes, insomnia, and other indications. The present invention also relates to pharmaceutical compositions comprising COMPOUND I or a pharmaceutically acceptable salt thereof.
CN103665082A Hemsleya cucurbitane tetracyclic triterpenoid compound, pharmaceutical compositions containing same and application of compound and pharmaceutical composition The invention relates to a Hemsleya cucurbitane tetracyclic triterpenoid compound with a structural formula (I) which is described in the specification. In the structural formula (I), R1 is H and R2 is H; or, R1 is beta-D-Glc, and R2 is Ac. The invention further relates to a pharmaceutical composition with the compound as an active component and application of the compound and the pharmaceutical composition in drugs used for treating lung adenocarcinoma and colorectal carcinoma.
US20110217265 Screening for Inhibitors of HCV Amphipathic Helix (AH) Function Screening methods are provided for identifying pharmacologic inhibitors of HCV amphipathic helix (AH) function, which inhibitors are useful in the prevention and treatment of HCV infection. Also provided are compounds useful in the inhibition of viral replication. The methods of the invention are based on the unexpected discovery that the presence of an AH, e.g. an AH of an HCV polypeptide, causes an increase in the apparent diameter of the vesicles. The methods of the invention provide for addition of AH peptides to lipid vesicles, for example in a high-throughput format; which addition may be performed in the absence or presence of a candidate pharmacologic agent. The change in apparent vesicle size is measured, and compared to control samples. An increase in vesicle size or aggregation is indicative of AH function being present; and a lack of increase is indicative that the AH function is absent or has been inhibited by a test agent.
CN103554213A 4-oxa-androstane-3-ketone-17beta-amides derivatives, as well as preparation method and medical applications thereof The invention relates to the field of medicinal chemistry, and particularly relates to 4-oxa-androstane-3-ketone-17beta-amides derivatives of a general formula I, as well as preparation methods and medical applications of the derivatives. The compounds, namely the derivatives, can be used for treating various human endocrine diseases such as benign prostatic hyperplasia, prostatic cancers, alopecia, acne and hirsutism which are mainly caused by dihydrotestosterone. The general formula I is shown in the specification.
CN101253270A Prophylactic/ameliorating agent for menopausal disorder and functional beverage/food Disclosed is a method for producing an estrogen-like active intermediate (e.g., secoisolariciresinol) by culturing a lignan (e.g., a lignan derived from Gymnema sylvestre) together with a bacterium Lactobacillus acidophilus. Also disclosed a prophylactic/ameliorating agent for menopausal disorder and a functional beverage/food for preventing/ameliorating menopausal disorder comprising a lignan cultured together with a bacterium Lactobacillus acidophilus as an active ingredient.
WO2006050126A1 Hypoestoxides, derivatives and agonists thereof for use in the treatment and prophylaxis of obesity Methods of treating a host suffering from obesity or an overweight condition are provided. Methods of preventing obesity or an overweight condition are also provided. The methods include delivery of a hypoestoxide, hypoestoxide derivative or hypoestoxide agonist, or hypoestes dried leaf powder to a host suffering from obesity or an overweight condition or a host at risk for developing obesity or becoming overweight. The methods further include the administration of a chemotherapeutic agent, such as a non-steroidal anti-inflammatory drug, in combination with delivery of a hypoestoxide, hypoestoxide derivative or hypoestoxide agonist, or hypoestes dried leaf powder.
US20090104237 Method for increasing tissue oxygenation Disclosed are methods and compositions for increasing tissue oxygen levels by administration of superoxygenated compositions of tissue surfaces. The methods are applicable to treatment of a wide variety of conditions including burns, bedsores, ulcers, necrosis and anaerobic infections.
US7015252 comprises ubiquinones; decreasing amount of urinary 8-hydroxydeoxyquanosine in diabetic animals The present invention provides an antioxidative composition with high safety, which is capable of lessening oxidative stress due to active oxygen species, free radicals, or the like in vivo, thereby preventing the occurrence or worsening of a disease. It was confirmed that by using a composition containing oxidized coenzyme Q and/or reduced coenzyme Q, the amount of urinary 8-hydroxydeoxyquanosine can be decreased in normal or diabetic animals. Also, in histopathological research of the spleens of diabetic rats, it was confirmed that spleen tissue denaturation caused by oxidative stress can be prevented. It was thus found that oxidative stress in vivo can be lessened. According to the present invention, oxidative stress in vivo can be lessened by using a composition containing coenzyme Q as an active ingredient.
WO2012053741A2 Nucleic acid molecules inducing rna interference, and uses thereof The present invention relates to nucleic acid molecules having a novel structure which induce RNAi, and to the uses thereof. More particularly, the present invention relates to nucleic acid molecules which have a novel structure and which increase the rate of inhibiting the expression of target genes by configuring the structure to have a first strand of 24-121 nt in length provided with a partial region complementary to a target nucleic acid, and a second strand of 13-21 nt in length provided with a region which forms a complementary bond with the partial region complementary to the target nucleic acid of the first strand. The invention further relates to a method for inhibiting the expression of the target genes using the nucleic acid molecules. The nucleic acid molecular structure according to the present invention can increase a gene inhibition rate, or increase the inhibition rate of the target genes by improving the bonding strength to the same target genes together with siRNA through the introduction of antisense DNA, antisense RNA, ribozyme, and DNAzyme, or by causing synergistic cleavage. Furthermore, the nucleic acid molecules according to the present invention enables the continuance time of a gene inhibition rate to be lengthened. Thus, the nucleic acid molecules inducing RNAi are useful since they replace the conventional siRNA molecules applicable to the treatment of cancer or of viral infection using siRNA.
CN1784993A Method for preparing sour soymilk contg. micron ginseng, antler pearl and pollen pini for tonifying-Yang, dispelling-fatigue and enriching-calcium A micron-class health-care sour bean milk for invigorating Yang, relieving fatigue and supplementing Ca is prepared from traditional bean milk, micron-particles of ginseng, antler, pine pollen and pear, oligose and useful intestinal bacteria through proportional mixing, processing and fermenting. Its advantages are high effect and rich nutrients including vitamins, minerals, etc.
US20120244108 Compositions And Methods For Separating Tissue In one aspect, methods for separating biological tissue are described herein. In some embodiments, a method for separating tissue comprises providing a first composition comprising a polymerizable material, providing a second composition comprising a polymerization initiator, disposing the first composition at a first site beneath a first tissue layer, disposing the second composition at the first site, polymerizing the polymerizable material at the first site, and separating the first tissue layer from a second tissue layer.
WO2009142594A9 The use of 3beta-ethenyl, methyl, 3alpha-hydroxy-steroids for the treatment of cns disorders Compounds exhibiting 3alpha-hydroxy-delta 4-5, 5alpha/beta-steroid blocking action with no or only low antagonism against the gamma-aminobutyric acid (A) receptor (GABA-A) are presented. Methods for the prevention, treatment and/or alleviation of various CNS-disorders are suggested, as well as pharmaceutical compositions for such use.
CN102973582A Compound florfenicol and neomycin sulfate nanoemulsion formulation and preparation method thereof The invention belongs to the field of veterinary medicine, and in particular relates to a compound florfenicol and neomycin sulfate nanoemulsion formulation with high stability and a good absorption effect and a preparation method thereof. The nanoemulsion formulation is of oil-in-water type with a particle size of 1-100 nm, and is prepared from florfenicol, neomycin sulfate, a cosolvent, a surfactant, a cosurfactant, oil and distilled water. The invention is simple in preparation process, low in production cost, good in drug absorption effect, and improved in drug utilization; the method uses nanoemulsion as a drug carrier; and the formulation has the advantages of broad spectrum, efficiency, target, sustained release, security, etc. and is significant in the effect of treatment of bacterial infection.
CN101491532B Erigeron breviscapus eye-preparation and preparation method thereof The invention discloses an erigeron phenol ophthalmic preparation and a preparation method thereof. The ophthalmic preparation comprises an eye drop, an ophthalmic liposome, an inclusion complex eye drop, an eye ointment, ophthalmic in situ-gel, and the like. The ophthalmic preparation is prepared by taking erigeron phenol as an active effective constituent and adding pharmaceutical expicients ofthe ophthalmic preparation, and the like, the weight percentage of the contained erigeron phenol is between 0.1 and 30 percent, and the balance is the pharmaceutical expicients of the ophthalmic preparation. The erigeron phenol is applied to the ophthalmic preparation, and has the advantages that compared with the prior erigeron whole-grass extract preparation, the erigeron phenol dispels impurities, has high purity of the active effective constituent, and can meet the need of the preparation of the ophthalmic preparation, when prepared into the ophthalmic preparation, the erigeron phenol increases the effective absorption of a medicine improves the bioavailability of the medicine, and increases the stability of the preparation. The ophthalmic preparation has better application prospect to the prevention and treatment of ophthalmic diseases, particularly the treatment of glaucoma disease.
WO2013015519A1 Antioxidant composition containing isorhamnetin-3-glucoside-7-rhamnoside separated from hippophae rhamnoides leaves as an active ingredient The present invention relates to an antioxidant composition containing isorhamnetin-3-glucoside-7-rhamnoside (IGR) separated from Hippophae rhamnoides leaves as an active ingredient. The IGR compound separated from the extract of Hippophae rhamnoides leaves according to the present invention has antioxidant, antibiotic, anti-cancer, and anti-inflammatory effects, and therefore may be valuably used as a cosmetic composition for preventing or reducing aging, as an antioxidant health food composition, as an antibiotic pharmaceutical composition, as a pharmaceutical composition for preventing or treating cancer, as a health food composition for preventing or ameliorating cancer, as a pharmaceutical composition for preventing or treating inflammation, and as a health food composition for preventing or ameliorating inflammation.
WO2009020534A2 Method of treating cxcr3 mediated diseases using heterocyclic substituted piperazines The present application discloses a method of treating a CXCR3 chemokine receptor mediated disease selected from the group consisting of chronic obstructive pulmonary disease (COPD), asthma, sarcoidosis, systemic lupus erythematosus (SLE), alkylosing spondylitis, fibrotic diseases, pulmonary fibrosis, alopecia areata, scleroderma, lichen planus erythematosus, discoid lupus erythematosus, dermatomyositis, Behcet's disease, Wegener's disease, atopic dermatitis, and graft-vs-host disease (GVHD) in a patient in need of such treatment comprising administering to the patient a therapeutically effective amount of at least one compound having the general structure shown in Formula 1: Formula 1 or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein.
CN102558167A Thiazolidine derivant with GK and PPAR double excitation activity The invention discloses a novel thiazolidine derivant and a preparation method, a medicine combination and a purpose thereof, which specifically relate to the thiazolidine derivant shown as the formula I and the formula II, officinal salt of the derivant, a precursor or a derivant with the same biological function with the thiazolidine derivant, the preparation method of the thiazolidine derivant, the combination of one or a plurality of thiazolidine derivants and the purpose of the compound in treatment on diseases related with glucokinase and a peroxisome proliferators activated receptor, such as diabetes mellitus and obesity.
CN1726916A Oral disintegration tablet for dropping blood sugar and preparation method An orally disintegrating hypoglycemic tablet is prepared from glipizide, filler, disintegrant, flavouring, lubricant and adhesive. Its advantage is short disintegrating time (less than 60 S). Its preparing process is also disclosed.
CN101863894A Tanshinone II A derivative and preparation method and application thereof The invention discloses a tanshinone II A derivative and a preparation method and application thereof. The structural formula of the tanshinone II A derivative is as shown in Formula (I). The preparation method adopts tanshinone II A and aldehydes for synthesis and has the advantages of safe and simple operation and high yield. The tanshinone II A derivative has a function of inhibiting the growth of tumor cells, can be applied in preparation of anti-tumor drugs and has potential value for industrial development and great significance for research and development of anticancer drugs.
US6872743 Antiinflammatory agents; sepsis shock; antiarthritic agents A novel class of tetracyclic compounds represented by the formula I wherein R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, and n are as defined is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
EP2621906A1 Diazaridine derivatives for treating metal disorders The present invention relates to compounds of formula (I) or (la), use of these compounds to treat mental disorders, especially depressions of different etiology, and methods for their preparation. The compounds that are provided for the treatment of mental disorders can be presented by a general formula (I) as meso-form -S,2S,1'R,2'R-1-[ω-(3,3-dialkyldiaziridin-1-yl)alkyl] -3,3-dialkyldiaziridines: wherein R, X and n are as defined in specification or pharmaceutically acceptable salts thereof, solvates thereof such as hydrates, and pharmaceutical compositions containing such compounds, with the proviso that the compound of Formula (I) is not meso-1S,2S,1'R,2'R-1-[2-(3,3-dimethyldiaziridin-1-yl)ethyl]-3,3-dimethyldiaziridine (R=Me, X=CH2, n=2) (Formula la).
CN101797379A Combination humidifying liquor for ultrasonic atomization therapy The invention discloses combination humidifying liquor for ultrasonic atomization therapy, which is characterized by respectively loading the following components of the liquor by content into respective bottles, further loading the bottles into a box provided with disposable syringes and packaging in an integral and plate-type way: 15ml to 25ml of physiological saline solution, 4mg to 6mg of dexamethasone, 4mg to 6mg of a-chymotrypsin and other liquor. When in use, the combination humidifying liquor can greatly save the time for a clinician to give a prescription and for a nurse to fill the prescription and prepare the liquor, avoid the trouble and error in temporarily filling the prescription and overcome the difficulties in incomplete drug combination, low portability and complex package and transportation frequently, and the like caused in clinical application. Therefore, the invention is suitable for not only large hospitals, but also community outpatient clinics, rehabilitation clinics and family-care wards.
WO2014052313A1 Topical ketoprofen composition A topical composition, specifically an oil-in-water emulsion, comprised of ketoprofen and oxybenzone in a physiologically acceptable topical carrier. The composition is applied topically to alleviate pain, especially pain associated with migraine headache. The composition has good photostability as well as freeze/thaw stability.
CN101108193A Water-solubility rutoside and method of manufacturing the same and oral preparation The invention discloses a water-soluable rutin preparation method, which is characterized in that: dissolve the rutin in organic solvent, add urea or polyethyleneglycol, heat the rutin, crystallize after the backflow, filter and dry up to get the water-soluable rutin. The invention also discloses a rutin oral formulation prepared with effective dosage of water-soluable rutin and pharmaceutically acceptable carrier supplementary materials. The rutin-urea or rutin- polyethyleneglycol associated matter changes the form of rutin from plane structure to a cubic structure, thus enhancing the water-solubility of rutin, improving the solubility of rutin in water, ensuring regular absorption and enhancing the biologic utilization rate of rutin in comparison with ordinary rutin tablet.
US8044206 Nitrogen—containing heterocyclic derivatives having 2,6-disubstituted styryl The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.
US20110190226 C4'-substituted-2-deoxyadenosine analogs and methods of treating hiv The invention provides for novel 2-Deoxyadenosine compounds, which can treat HIV infection at low cytotoxicity values. Substitution at the 4′-position provided compounds which demonstrated low cytotoxicity values in an ATP-based cytotoxicity assay.
CN101129678A Externally used formulated product for treating empyrosis and method of preparing the same The invention relates to an external-used pharmaceutical composition for treating burns and scalds and process for preparation, wherein the composition is prepared from the following raw materials (by weight portion): Chinese angelica root 5-10 parts, rhizome of Sichuan lovage 5-10 parts, safflower 6-18 parts, asarum herb 2-10 parts, frank incense 4-13 parts, dragon's blood resin 5-9 parts, root of Chinese trichosannthes 5-10 parts, astragalus root 5-10 part, myrrh 3-10 parts, borneol 1-3 parts, camphor 1-3 parts, iodine 50-150 parts and right amount of vaseline. The composition can be prepared from the herbs through water grilling, and directly disintegrating part of the medicinal raw materials and mixing with medicinal soups.
CN103394001A Specific medicine for curing beriberi and preparation method thereof The invention discloses a specific medicine for curing beriberi and a preparation method thereof. The specific medicine is prepared from the following raw materials by weight ratio: 5%-10% of realgar, 1%-3% of fructus cnidii, 2%-5% of aloes, 3%-6% of garlic, 5%-8% of flos rhodoendri Mollis, 4%-6% of folium artemisiae argyi, 10%-15% of sulphur, 13%-17% of radix stemonae, 6%-10% of acalypha australis, 8%-12% of borax, 2-10 parts of fish oil, 1-5 parts of borneol, 1-3 parts of white vaseline, 1-3 parts of radix angelicae pubescentis, 4%-8% of camphor, 8%-12% of gallnut and 1%-5% of borneol. The specific medicine disclosed by the invention has obvious treatment effect, can be used for radically curing the beriberi and has the advantages of no toxic or side effect, strong medicine property and quick acting, is capable of treating both manifestation and root cause of beriberi and inhibiting recrudescence and is prepared simply with low cost.
WO2013143663A1 Bicyclic pyrazinone derivatives Compounds of the formula (I) in which R1, X and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
WO2011014613A2 Preparation of fipamezole The application relates to processes for preparing fipamezole and its pharmaceutically acceptable salts, and intermediates thereof. It also provides intermediate compounds of Formula III and Formula IV, and processes for their preparation.
WO2006133837A3 A process for the preparation of an injectable solution of (2s)-n-(2;6-dimethyl-phenyl)-1-propyl-2-piperidincarboxamide A process for the preparation of an injectable solution of (2S)-(-)-N- (2;6-dimethyl-phenyl)-l-propyl-2-piperidincarboxamide (Ropivacaine) starting from Ropivacaine base substantially free from the dextro enantiomer, by dissolution of the same in water for injectables containing hydrochloric acid in stoichiometric amounts.
CN101618026B Meloxicam tablet, production technology and purposes thereof The invention discloses a Meloxicam tablet, a production technology and purposes thereof. The Meloxicam tablet consists of Meloxicam, lactose, pregelatinized starch, low-substitute hyprolose, polysorbate 80, 12% of pregelatinized starch for flushing syrup, superfine silica gel powder, magnesium stearate, alcohol and gastric-solubility film coating premixer. The production method of the Meloxicam tablet comprises the following steps: manufacturing tablet cores and coatings, and the like. The Meloxicam tablet treats 125 cases of rheumatoid arthritis, and the anti-inflammatory and pain-relievingcurative effects are good, while the curative effect on blood sedimentation is little, and the total effective rate achieves 84%. The invention has the characteristics of few medical taking times, stable blood and medicine concentration, long duration period, and the like.
US20110224159 Bidesmosidic betulin and betulinic acid derivatives and uses thereof as antitumor agents The instant application is directed to bidesmosidic betulin and betulinic acid saponin derivatives of formula (I), and use thereof as antitumor agents. In particular, said compounds are effective in treating lung carcinomas, colorectal adenocarcinomas, breast adenocarcinomas, and prostate adenocarcinomas. Methods of synthesizing said compounds through selective glycosylation of the C-28 and C-3 position, and diagnostic methods for identifying tumours suitable for treatment by said compounds are also disclosed.
US7973077 Amino acid based compositions for the treatment of pathological conditions distinguised by insufficient mitochondrial function The present invention relates to compositions suitable for the treatment of pathological conditions distinguished by insufficient or reduced mitochondrial function. The compositions comprise, as principal active ingredients, the amino acids leucine, isoleucine and valine. The compositions may also comprise, as further active ingredients, amino acids threonine and lysine, and optionally, histidine, phenylalanine, methionine, tryptophan, as well as tyrosine and cysteine.
US6930092 Antibiotic agents Methods of treating a microbial infection comprising administering to a patient in need of such treatment are disclosed. In one aspect the method comprises administering to a patient in need of such treatment a therapeutically effective amount of Erythromycin B (or a pharmaceutically acceptable derivative thereof). In another aspect the method comprises a pharmaceutical composition comprising at least 50% by weight of Erythromycin B (or a pharmaceutically acceptable derivative thereof) of the total weight of antibiotic present in the composition. Also disclosed are 2′-esters of Erythromycin B and Erythromycin B enol ether.
EP1593683A2 Dihydro-2,3-Benzodiazepine derivatives Compounds having general formula (I) wherein R is hydrogen or C1 - C10 alkyl; X is an aromatic moiety selected from phenyl, thienyl, furyl, pyridyl, imidazolyl, benzimidazolyl, benzothiazolyl and phthalazinyl which is unsubstituted or substituted with one or more moieties chosen from the group consisting of halogen, hydroxy, cyano, nitro, C1 - C6 alkyl, C3 - C6 cycloalkyl, C1 - C4 alkoxy, carboxy, C1 - C6 alkoxycarbonyl, acetyl, formyl, carboxymethyl, hydroxymethyl, amino, aminomethyl, methylenedioxy and trifluoromethyl; and "Aryl" represents p-nitrophenyl, p-aminophenyl or p-(protected amino) phenyl; or a pharmaceutically acceptable salt thereof, are useful as anticonvulsants.
WO2014087367A3 Compositions and methods for the treatment of neurological diseases and its associated complications The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurologic diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, seizures, mental diseases, mental disorders, schizophrenia, depression, bipolar disorder, Alzheimer's disease, anxiety, ADHD, dementia, mood disorders, PTSD, sleeplessness, epilepsy, migraine, psychosis, OCD, autism, anxiety disorders, dementia, mania and cognitive disorders.
US20110110951 Isolation of five novel genes coding for new fc receoptrs-type melanoma involved in the pathogenesis of lymphoma/melanoma This invention provides an isolated nucleic acid molecule which encodes immunoglobulin receptor, Immunoglobulin superfamily Receptor Translocation Associated, IRTA, protein. Provided too, are the IRTA proteins encoded by the isolated nucleic acid molecules, IRTA1, IRTA2, IRTA3, IRTA4 or IRTA5 proteins, having the amino acid sequences set forth in any of FIG. 18A, 18B-1-18B-3, 18C-1-18C-2, 18D-1-18D-2 or 18E-1-18E-2. Oligonucleotides of the isolated nucleic acid molecules are provided. Antibodies directed to an epitope of a purified IRTA1, IRTA2, IRTA3, IRTA4 or IRTA5 proteins are also provided, as are pharmaceutical compositions comprising such antibodies or oligonucleotides. Methods for detecting a B cell malignancy in a sample from a subject; diagnosing B cell malignancy in a sample from a subject; detecting human IRTA protein in a sample; and treating a subject having a B cell cancer are also provided.
WO2013022927A3 Treatment of uterine leiomyomata Embodiments herein provide a therapy for uterine leiomyomata (UL) in women using a fatty acid synthase (FAS) inhibitor. Additionally, an analysis method for evaluating the likelihood of women developing UL during their lifetime is provided.
CA2792417A1 Agomelatine hydrochloride hydrate and preparation thereof An agomelatine hydrochloride hydrate of formula (I), preparation, use, and pharmaceutical composition thereof are provided. Said hydrate obtained through the present method has significant increased solubi1ity than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. Using the present method, high purity can be obtained through a simple process, free of any complicated steps. Wherein X is Cl.
WO2013116823A1 Benzimidazoles and uses thereof The present invention relates to novel 2,5,6-benzimidazole derivatives of formula I and pharmaceutically acceptable salts thereof. Another aspect of the invention relates to methods of treating a patient infected by Mycobacterium tuberculosis or Mycobacterium avium complex by administering to the patient a 2,5,6- benzimidazole derivative or a pharmaceutically acceptable salt thereof.
EP2417446A1 A method of characterizing phytochemicals from trigonella foenum graceum The present invention relates to identification and characterization of Phytochemicals and metabolites from Trigonella foenum-graecum extract by Liquid chromatography and Mass spectrometry LC-MS/MS.
CN101310726A Alcohol-containing polyhexamethylguanidine iodine disinfectant and preparation method thereof The invention relates to a disinfectant, in particular to the rapid skin disinfectant and a preparation method thereof. The alcohol-containing PHMG iodine disinfectant comprises components with the following percentages by weight: 0.05 to 2 percent of PHMG; 0.1 to 5 percent of iodine; 30 to 80 percent of alcohols; 0.1 to 2 percent of stabilizer; 0.1 to 1 percent of penetrating agent; 0.1 to 2 percent of skin care agent; 0.1 to 0.8 percent of phosphoric acid with the concentration of 10 percent and the rest of water. The preparation method of the alcohol-containing PHMG iodine disinfectant is that: the PHMG and the iodine are added in the alcohol according to the components and the contents of the disinfectant, the mixture is heated and mixed for 0.5 to 2 hours at the temperature of 30 to 70 DEG C, the stabilizer, the penetrating agent, the skin protective agent and the phosphoric acid of 10 percent are then respectively added, the water is finally added to 100 percent to be evenly mixed, and the disinfectant is obtained. The disinfectant has strong sterilization ability and very high stability, and the effective period is as long as two years, thus being the ideal rapid skin disinfectant.
US20090270499 Process for Synthesizing Atazanavir This invention relates to a process for synthesizing Atazanvir, including novel intermediates and novel steps to various intermediates along the synthetic pathway.
US20090156664 Natural Vitamin E Compositions with Superior Antioxidant Potency Compositions for increased antioxidant potency of natural vitamin E (d-alpha-tocopherol), comprising alpha-, beta-, delta-, and gamma-forms of tocopherols and tocotrienols are disclosed. All of these compositions provide 400 International Units (IU), based on one mg of d-alpha-tocopherol provides 1.49 IU. These compositions showed antioxidant activities superior to natural d-alpha-tocopherol. These compositions are designed to provide protection of the cell membrane lipid layer, and protection against heart disease, cancer, and eye disease.
CN101596211A Drug combination for reducing blood sugar and lipid levels A drug combination for reducing blood sugar and lipid levels comprises berberine, vitamin B complex, vitamin E and trace elements such as zinc, selenium, chromium, copper, molybdenum, iodine and manganese. The drug combination is mainly suitable for the population suffering from high blood sugar and lipid levels, has good effects on reducing blood sugar and lipid levels and can be taken for long term or according to the courses of treatment.
US7341739 Small particle liposome aerosols for delivery of anti-cancer drugs The small particle liposome aerosol compounds and methods of treatment of the present invention involve lipid- or water soluble anti-cancer drugs incorporated into liposomes. The liposomes are administered in aqueous dispersions from a jet nebulizer to the respiratory tract of an individual. Various anti-cancer drugs may be used, including 20-S-Camptothecin, 9-Nitro-camptothecin, 9-Amino-camptothecin, 10, 11-methylenedioxy-camptothecin and taxol or its derivatives. Administration of these drugs by inhalation provides faster and more efficient absorption of the anticancer drug than does intramuscular administration or oral administration.
US7214687 Quinuclidine derivatives and medicinal compositions containing the same The invention provides 3 (R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1 -azoniabicyclo[2.2.2]octane in salt form, pharmaceutical compositions comprising it, and methods of using it for treatment of respiratory disorders, in association with phosphodiesterase 4 inhibitors.
CN103393669A Application of Chukrasone B in medicament for preventing pancreas fibrosis The invention discloses an application of Chukrasone B for preparing a medicament for preventing and treating pancreas fibrosis. The application of Chukrasone B for preparing the medicament for preventing pancreas fibrosis is firstly disclosed. Because a matrix type belongs to a new matrix type, and Chukrasone B has unexpectedly strong inhibition activity on pancreas fibrosis without possibility of any enlightenment given by other compounds, Chukrasone B has significantly substantive characteristics, and simultaneously has substantial progress for resisting pancreas fibrosis.
WO2010022380A2 Linear polyol stabilized polyfluoroacrylate compositions The present invention is directed to compositions of a linear polyol and a salt of a crosslinked cation exchange polymer comprising a fluoro group and an acid group. These compositions are useful to bind potassium in the gastrointestinal tract.
EP1827417A4 Enhanced occlusive effect photodynamic therapy This invention discloses methods of treating neovasculature diseases of the eye through the administration of a photosensitizing agent and subsequent exposure to light of specific wavelength sufficient to photoactivate the photosensitizing agent to occlude one or more vessels in the neovasculature for an extended period of time. Diseases treatable under this invention, include, for example: diabetic retinopathy; macular degeneration; subfoveal choroidal neovascularization, malignant uveal melanomas and other maladies of the human or animal eye or body.
US20080226700 Containing allantoin and plant extracts; skin disorders; antiulcer agents The present invention relates to a medicated gauze containing as active ingredient, aliantoin, a Centella Asiatica extract and, optionally, an Urtica dioica extract.
US20080227782 Pyrimidine amide compounds as pgds inhibitors This invention is directed to a compound of formula (I): wherein R1, R2, R3 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).
US20120190663 Use of free dna as an early predictor of severity in acute pancreatitis This invention provides methods of determining the risk of AP development in an individual, as well as the diagnosis, prognosis, and treatment of acute pancreatitis (AP) in an individual, by determining the presence or absence of significantly high levels of free serum DNA in the subject relative to levels in a healthy individual. In other embodiments, the invention further provides methods of determining the risk of severe AP development, prognosis, diagnosis, and treatment of a severe form of acute pancreatitis based upon the presence of significantly high levels of free serum DNA in the subject relative to an individual who has and maintains a mild form of acute pancreatitis.
CN1935265A Grafted nano carbon anticancer prodrug, and its preparing method and use The present invention relates to a graft nano carbon anticancer pro-drug, its preparation method and application. Said graft nano carbon anticancer pro-drug is made up by coupling graft nano carbon with anticancer drug. Said invention also provides its chemical structure formula, and said graft nano carbon anticancer pro-drug can effectively cure or inhibit lymphogenous metastasis of cancer cell.
CN102786434A Acetaminophen acid derivative, preparation method and application thereof The invention relates to an acetaminophen acid derivative, a preparation method of the acetaminophen acid derivative and the application of the acetaminophen acid derivative, and belongs to the technical field of organic synthesis. The acetaminophen acid derivative has a structural formula shown in the specification, wherein if R2=R3=H, R1 is F, Cl, Br, CH3, OCH3, NO2 and H; if R1=R3=H, R2 is F, Cl, Br, CH3, OCH3 and NO2; and if R1=R2=H, R3 is F, Cl, Br, CH3, OCH3 and NO2. The acetaminophen acid derivative provided by the invention not only has relatively high antitumor activity, can be applied for preparing antitumor drugs, and but also has simple and easy preparation method, and the preparation method is easy to operate.
CN101072765A Phenylpiperazines with a combination of affinity for dopamine -D2 receptors and serotonin reuptake sites The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine -D2 receptors and to methods for the preparation of these compounds. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula ( 1 ) wherein the symbols have the meanings given in the specification.
CN102574782A Substituted halophenoxybenzamide derivatives The present invention relates to substituted halophenoxybenzamide derivative compounds of general formula (I) in which R1, R2, R3, R3a, R4, R5, R6, Ra, Rb, Rc, and X are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
CN1993331A N- (1- (1-benzyl -4-phenyl-1h-imidazol-2-yl) -2,2-dymethylpropyl) benzamide derivatives and related compounds as kinesin spindle protein (ksp) inhibitors for the treatment of cancer This invention is directed to substituted imidazole compounds which modulate the activity of KSP and are useful for the treatment of cancer and are represented by the formula (I) wherein: R1 is selected from the group consisting of aminoacyl, acylamino, carboxyl, carboxyl ester, aryl, and alkyl optionally substituted with hydroxy or halo; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; R3 is selected from the group consisting of hydrogen and -X-A, wherein X is selected from the group consisting of-C(O)-, -C(S)-, -S(O)-, -S(O)2-, and -S(O)2-N(R)-, where R is hydrogen or alkyl; and A is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted aryl, carboxyl, carboxyl ester, aminoacyl, optionally substituted heteroaryl, optionally substituted heterocyclic, and optionally substituted cycloalkyl, wherein the optionally substituted groups are substituted with 1 to 4 substituents; R5 is selected from the group consisting of L-A1, wherein L is selected from the group consisting of-S(O)q- where q is one or two, and C1 to C5 alkylene optionally substituted with hydroxy, halo, or acylamino; and A1 is selected from the group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, cycloalkyl, and substituted cycloalkyl; and one of either R6 or R7 is selected from the group consisting of heterocyclic, aryl and heteroaryl, all of which may be optionally substituted with -(R8)m where R8 is as defined herein and m is an integer from 1 to 3, and the other Of R6 or R7 is selected from the group consisting of hydrogen, halo, and alkyl; or R6 and R7 are both hydrogen; the other substituents are defined in the claims.
USRE40794 Antibiotic product for therapy of infections; purification for improved purity and stability A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than −5° C., c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a C2-5 alcohol at between −5 and −25° C.
CN101108190A Application of cryptotanshinone in preparation of medicine preventing and controlling autoimmune disease The invention discloses the application of cryptotanshinone in preparing drug that prevent and treats autoimmune disease, in particular to the application for preparing the drug that prevents and treats rheumatoid arthritis. The drug can be prepared in the mode of oral solution, injection or external application formulation. The cryptotanshinone in the invention has the advantages of excellent curative effect, high cure index, safe application and little toxic and side effect.
WO2007145326A1 Method for determination of inflammatory disease The object is to provide: a method for the determination of an inflammatory disease including cardiac infarction, which is characterized by identifying a gene polymorphism involved in cardiac infarction and utilizing the gene polymorphism; an oligonucleotide which can be used in the method; a kit for the diagnosis of an inflammatory disease; a therapeutic agent for an inflammatory disease; and others. Disclosed is a method for the determination of an inflammatory disease, comprising detecting at least one gene polymorphism found in proteasome subunit α type-6 gene.
CN102357129B Fishbone calculus-dissolving decoction for treating lithiasis The invention relates to a fishbone calculus-dissolving decoction for treating lithiasis, which can effectively solve the medicament problem of lithiasis treatment; the decoction is prepared by water and the following components: 18-20 g of talcum, 14-16 g of lygodium japonicum, 14-16 g of white peony roots, 14-16 g of chicken gizzard membrane, 9-11 g of mirabilite, 11-13 g of rhizoma corydalis, 9-11 g of licorice, 1.2-1.4 g of otolhum pseudoscinaenae, 28-32 g of wild amaranthus spinosus, and 28-32 ml of vinegar; the mirabilite is firstly processed by a method comprising the following steps: cleaning and cutting radishes into pieces, completely boiling with water, adding mirabilite, boiling together till the mirabilite are dissolved completely, filtering or clarifying the solution, pouring out the upper liquid, cooling to precipitate the mirabilite; the decoction is prepared by drying the processed mirabilite, mixing with talcum, lygodium japonicum, white peony roots, chicken gizzard membrane, rhizoma corydalis, licorice, otolhum pseudoscinaenae, and wild amaranthus spinosus, decocting the mixture with water for three times with the amount of the added water being 800-1200 ml for each time and decocting time being 30-60 min for each time, combining the three decoctions, adding vinegar, well mixing to obtain the fishbone calculus-dissolving decoction; the invention has scientific formulation, abundant raw materials, is easy to prepare, convenient for administration, has good effect, and low cost; no surgical operation is required for calculus removal, which reduces patient pain.
CN1683340A 2-nitro-gen-dicyclic [2, 2, 1] hepta-5-ene-3-carboxylic derivative and its use preparing neuro regulator The present invention relates to substituted 2-nitrogen-dicycle [2.2.1] heptyl-5-ene-3-carboxylic derivatives and their medicinal salt and hydrates with nerve nourishing effect, their medicine compositions, and their use as FK506 conjugated proteinase activity inhibitor in medicine for preventing and treating neutrodegrneation disease and other diseases caused by nerve damage or relevant diseases.
CN102443045A N-substituted phenyl-14 beta -(aminomethyl) triptodiolide derivative and preparation method and application thereof The invention provides a tripterygium diterpenoid lactone derivative shown in Formula II-5 or a pharmaceutically acceptable salt thereof, a preparation method thereof, a drug combination thereof and an application thereof in preparation of drugs for treatment of tumors, in particular to ovarian cancer or prostate cancer.
CN101274913A Ornidazole sodium succinate compound, medicinal composition and use thereof The invention relates to a new compound, ornidazole succinate sodium and combinations and a preparation method thereof. The ornidazole succinate sodium not only has excellent water solubility and stability but also both in vitro experiment and in vivo experiment shows similar efficacy to the prior art with respect to showing fungistatic action, and has better anti-trichomonad function and less toxic and side effect compared with the prior art.
CN102552133A Middle/long chain triglyceride flurbiprofen axetil injection and preparation method thereof The invention provides anti-inflammatory and analgesic flurbiprofen axetil injection and a preparation method thereof. A mixture of 0.1-10 percent (w/v) of flurbiprofen axetil, 10-20 percent (w/v) of middle chain triglyceride (MCT) and 10-20 percent (w/v) of long chain triglyceride (LCT) is contained in the prescription (wherein the proportion of MCT and LCT is 4:1-1:4). The preparation method comprises the following steps: taking 1-5 percent (w/v) of lecithin as an emulsifying agent, taking 1-5 percent (w/v) of glycerol as an isotonic agent, finally adding disodium hydrogen phosphate, citric acid and water for injection and adjusting the pH value to 4-7 to prepare flurbiprofen axetil fat emulsion injection through colostrums, homogeneity and sterilization. The injection has the beneficial effects that the anti-inflammatory and analgesic effect is taken more quickly; the accumulation of fat of a human body can be reduced, and fatty tissues and liver load can be reduced; and the injection is more suitable for critically ill patients and people with poor liver functions and has lower toxic and side effects.
CN102558160A 4-substituted p-methyl sulfonamide anilino-quinazoline derivatives and preparation method and application thereof The invention belongs to the technical field of pharmaceutical chemistry, and relates to 4-substituted p-methyl sulfonamide anilino-quinazoline derivatives with a general formula (I), wherein R1 and R2 respectively have meanings limited in the specifications. The invention also relates to a preparation method of the derivatives, physiologically acceptable salt composed of the derivatives and inorganic or organic acid or alkali, and a pharmaceutical composition containing the same. The compound has valuable pharmacological properties, has an inhibitory effect on signal transduction caused by PTK (Protein Tyrosine Kinase), and especially has higher inhibitory activity on a mutant EGFR (Epidermal Growth Factor Receptor) (L858R/T790M) and an HER2 (Human Epidermal Growth Factor Receptor 2). The invention also relates to a method for treating diseases, especially diseases characterized by abnormal erbB family PTK activity, by using the derivatives.
WO2006039639A1 Crystalline forms and process for preparing spiro-hydantoin compounds A process is provided for preparing spiro-hydantoin compounds of the formula (II), wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G' is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula (II). The spiro-hydantoin compound of formula (II) and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S, 9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3- carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.
US7462623 Quinazoline derivatives as Src tyrosine kinase inhibitors The invention concerns quinazoline derivatives of Formula (I): (A chemical formula should be inserted here—please see paper copy enclosed herewith) wherein Z is an O, S, SO, SO2, N(R2) or C(R2)2 group wherein each R2 group is hydrogen or (1-8C) alkyl, m is 0, 1, 2 or 3, each R1 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, n is 0, 1, 2 or 3, and each R3 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, or pharmaceutically-acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumor disease.
WO2012178127A3 Site-activated binding systems that selectively increase the bioactivity of phenolic compounds at target sites The teachings provided herein generally relate to site-activated binding systems that selectively increase the bioactivity of phenolic compounds at target sites. The systems can include a phenolic compound bound to a reactive oxygen species, wherein the phenolic compound and the reactive oxygen species can react at a target area in the presence of an oxidoreductase enzyme. The systems can be used, for example, as an antitoxin, an anti-inflammatory, or an antimicrobial. Uses can include treatment of a gastrointestinal condition, a damaged dermal tissue, or a damaged mucosal tissue, as well as in promoting gastrointestinal health that can, for example, result in alleviating gastrointestinal discomfort or, perhaps, creating a weight gain in an animal.
US7485654 Corneal perception recovery drug containing amide compound The amide compound of the formula (I) [each symbol is as defined in the description] has a promoting action on neuritogenesis of trigeminal nerve cells, and the compound is useful as a corneal neuritogenesis promoter, an agent for recovering corneal sensitivity by promotion of corneal neuritogenesis, and an agent for treating dry eye.
WO2012088885A1 Total flavonoid extract of fructus aurantii immaturus or fructus aurantii, and use thereof A total flavonoid extract of Fructus Aurantii Immaturus or Fructus aurantii, obtained by extraction through decoction with water or extraction with ethanol under reflux and used in preparation of drugs for gastrointestinal motility disorders functional dyspepsia, epigastric pain, abdominal distension, anorexia, belching, nausea, vomiting, and pharmaceutically acceptable dosage form.
US20080214471 Method for inhibition of viral infection The invention is directed to inhibiting viral morphogenesis and viral infection. In particular, it concerns effecting such inhibition by inhibiting the prenylation or post prenylation reactions of a viral or host protein.
CN1976918A 4,5-disubstituted-2-aryl pyrimidines 4,5-disubstituted-2-arylpyrimidines of Formula (I) and Formula (II) are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.
US20100298444 Method for improving the therapeutic efficacy of curcuminoids and their analogs The invention relates to a method for increasing the therapeutic efficacy of curcuminoids and analogs. More specifically, the invention relates to a method for increasing the therapeutic efficacy of systemically administered formulations that contain curcuminoids and the equivalent therapeutics thereof. The method is characterized in that together with the administration of the formulation the patient is irradiated with visible, and optionally ultraviolet, radiation during a treatment. The invention also relates to phototherapy devices that emit visible radiation over a surface area greater than 0.2 m2 with an irradiance of more than 2 mW/cm2, the devices being suitable for use in the treatment of proliferative diseases, particularly moderate-to-severe psoriasis or tumor processes.
WO2008030141A1 Use of nifuroxazide in the form of a component of a combined drug therapy for treating diseases associated with helicobacter pylori and a curing method for eradicating a causative agent The invention relates to medicine, in particular to gastroenterology and is directed at treating diseases associated with the infection generated by Helibacter pylori and at eradicating said causative agent. The invention consists in using nifuroxazide in the form of a component of a combined drug therapy of gastrointestinal tract diseases associated with the Helibacter pylori infection, wherein said combined drug therapy is directed at eradicating the causative agent and contains nifuroxazide, a component for controlling acid-forming processes in a stomach and at least one additional antibacterial component, which is effectiveagainst Helibacter pylori, or tripotassium bismuth dicitrate. The invention also relates to a method which is used for treating diseases associated with the infection generated by Helibacter pylori, directed at eradicating said causative agent and consists in administering the invective components for combined therapy in a therapeutically effective quantity. The inventive curative method makes it possible to efficiently eradicate the causative agent, is alternatively low-cost with respect to applied therapeutic regiments of first-order therapy and practically does not causes secondary effects. The preferred embodiment of nifuroxazide is Enterofuryl in the form of a peroral suspension. The inventive method is particularly useful for treating children.
US20090029943 Glucosamine and Derivatives Thereof Useful as TG Inhibitors Disclosed herein is a transglutaminase inhibitor comprising glucosamine or a derivative thereof. Exhibiting potent inhibitory activity against transglutaminase, the overexpression of which is responsible for the etiology of various diseases, glucosamine or derivatives thereof can be useful in the prevention and treatment of such diseases. Also, a pharmaceutical composition comprising glucosamine or a derivative thereof as an active ingredient and a method of inhibiting transglutaminase are disclosed. Featuring the use of the pharmaceutical composition, the method can be therapeutically safely and effectively-applied to patients afflicted with such diseases.
EP1695707A1 Nail varnish containing tazarotene and use thereof for treating and/or preventing psoriasis Nail varnishes containing tazarotene (ethyl 6-[(3,4-dihydro-4,4-dimet hyl-2H-1-benzthiopyran-6-yl)ethynyl]-3-pyridine carboxylate) (I) are new. - ACTIVITY : Antipsoriatic; Dermatological. - MECHANISM OF ACTION : None given.
WO2014100501A1 Small molecule agonists of neurotensin receptor 1 Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
CN101006059A Substituted tetrahydroisoquinolines used in the form of MMP inhibitors, method for the production and use thereof in the form of drugs The invention relates to compounds of formula (I), wherein R1, R2, R3, R4, A, n and L have the significances indicated in the description. The use of the inventive compounds in the form of drags for preventing and/or treating diseases in which progression an active reinforced matrix-metalloproteinases take part is also disclosed.
US20080089881 Using nicotinic acid receptor (HM74) as diagnostic and evaluative tool in detection of psoraisis, ulcerative colitis, multiple sclerosis, irratable bowel and/or , crohn's diseases A method of determining whether a subject is suffering from or at risk for developing inflammatory diseases by determining the level of HM74 and/or HM74A in tissue damage. Also disclosed are a method of identifying a compound for treating inflammatory diseases, a method of treating inflammatory diseases, and a pharmaceutical composition or a packaged product for treating inflammatory diseases.
EP1549655A2 Substituted bicyclic thiophene derivatives, compostions containing such compounds and methods of use The present invention addresses substituted thiophene derivatives, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.
US20100048611 Tetrahydropyrrolopyridine, tetrahydropyrazolopyridine, tetrahydro-imidazopyridine and tetrahydrotriazolopyridine derivatives and use thereof The invention relates to novel tetrahydropyrrolopyridine, tetrahydropyrazolopyridine, tetrahydroimidazopyridine and tetrahydrotriazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders
US20060247310 Body temperature elevating agents The present invention provides body temperature elevating agents and foods and drinks for body temperature elevation. The invention relates to the body temperature elevating agent and food and drink for the body temperature elevation, which is comprised of medium chain fatty acid and/or glycerin fatty acid ester including the medium chain fatty acid, preferably medium chain fatty acid triglycerin as an active ingredient(s).
CN1634950A Clindamycin and metronidazole pessary The invention discloses a clindamycinum metronidazole pessary, preparation process and application thereof. The pessary uses salt or ester of clindamycinum and metronidazole as active constituent, and it comprises a water soluble suppository base polyethylene glycol composition which is formed by mixing polyethylene glycol 400, polyethylene glycol 1500 and polyethylene glycol 4000 in a proportion of 1:2:2. The preparing process is simple and reasonable. Cost is low, and the product quality is steady.
US7122618 Cosmetics, drugs, plant safening agents, microbiocides, textiles The present invention relates to quaternized polyamidoamines which have at least one structural unit of the formula VII in which R1, R2, R4 are straight-chain or branched organic radicals optionally containing heteroatoms; R5 is hydrogen or alkyl, R7 is hydrogen or alkyl or two radicals R7 together form a radical having a meaning given for R4, b is an integer from 0 to 50, and c is an integer from 1 to 50. The invention also relates to the preparation of the quaternary polyamidoamines, to compositions which comprise these compounds, and to the use thereof for cosmetic and pharmaceutical purposes, and in the fields of crop protection and textile dyeing. The present invention also relates to the use of quaternized polyamidoamines of the ionene type as biostatic or biocide and thus also biocidal compositions based on quaternized polyamidoamines.
WO2006064218A1 Hydantoin derivatives useful as metalloproteinase inhibitors Formula (I) wherein R1 is a (2-4C)alkyl and is substituted by two or more fluorine groups and R2 is methyl or ethyl, or a pharmaceutically acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by metalloproteinase enzymes.
CN1977844A Pioglitazone and glimepiride compound dropping pill preparation and its preparing method The present invention relates to a pyrrolidone and glimepiride compound dripping pills preparation and its preparation method. Its composition includes the mixture of pyrrolidone and glimepiride and matrix, and their weight ratio is 1:1.5-4.5.
US20070298026 Methods for Identifying Treatment and Inducing Infertility Using Smc1-Beta The present invention is directed to methods and compositions for use in the diagnosis and treatment of reproductive fertility. More particularly, it is directed to methods and compositions that can be used in male and female contraception and fertility.
WO2006097460A1 Hydroxamates as histone deacetylase inhibitors and pharmaceutical formulations containing them Compounds of structure (I) having histone deacetylase (HDAC) inhibitor activity are described. The compounds are chemically characterised by the presence of hydroxamic acid, with zinc as chelator, and an aromatic nucleus connected by a linker in which either a bicyclic aromatic system or a piperidino ring are present.
US7547705 Ethyl-1'-[(2S)-2-hydroxy-2-phenylethyl]-6'-oxo-8'-(pyridin-4-yl)-1',3',4',6'-tetrahydro-1H-spiro[piperidine-4,2'-pyrimido[1,2-a]pyrimidine]-1-carbox; glycogen synthase kinase-3 beta, amyloid precursor protein, tau protein hyperphosphorylation inhibitor; neurodegenerative disease, type II diabetes The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.
CN102199116A Fluoro imido sugar compounds, and preparation method and application thereof The invention provides fluoro imido sugar compounds, and a preparation method and application thereof. The structures of the fluoro imido sugar compounds provided by the invention are shown in formula (I) and formula (II), wherein n = 1 or 2; X is hydroxyl or fluorine; R1, R2 and R3 are selected from hydrogen, hydroxyl, hydroxymethyl, benzyl, benzyloxyl and benzyloxymethyl; R4 and R6 are selected from hydrogen, fluorine, methyl, methyl substituted with one to three fluorine atoms, hydroxymethyl, ethyl, hydroxyethyl, (1S)-hydroxyl hydroxyethyl, (1R)-hydroxyl hydroxyethyl, hydroethyl substituted with one to four fluorine atoms, propyl, butyl and phenyl substituted by one to five hydroxyl groups or methoxyl groups; R5 is hydrogen or C1-18 straight-chain or branch-chain saturated alkane; and R7 and R8 are hydrogen, fluorine, hydroxyl, methyl, ethyl, propyl, hydroxymethyl or trifluoromethyl. The preparation method of the fluoro imido sugar compounds provided by the invention is simple and efficient. The fluoro imido sugar compounds provided by the invention can be used as potential drugs for inhibiting glycosidase or resisting tumors.
CA2230556C Novel procollagens There is disclosed molecules comprising at least a first moiety having the activity of a procollagen C-propeptide and a second moiety selected from any one of the group of an alien collagen .alpha.-chain and non-collagen materials, the first moiety being attached to the second moiety. Also disclosed are collagen molecules, fibrils and fibres comprising a non-natural combination of collagen .alpha.-chains, DNA encoding same, expression hosts transformed or transfected with same, transgenic animals and methods of producing a non-natural collagen.
US7078438 N-(4 substituted phenyl)-anthranilic acid hydroxamate esters The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
US7256194 Compounds that inhibit factor Xa activity The present invention relates to compounds of the Formula or a pharmaceutically acceptable salt, solvate, hydrate or formulation thereof. These compounds can be used for the inhibition of Factor Xa and for the treatment and/or prevention of diseases that are mediated by Factor Xa activity.
EP2562257A1 Method for stabilizing functional nucleic acids This invention is intended to enhance and improve the resistance of a single- or double-stranded nucleic acid fragment comprising a base sequence of a functional nucleic acid to degradation by nucleolytic enzymes in a simple and cost-effective manner. The single- or double-stranded nucleic acid fragment comprises, ligated to at least one end thereof, hairpin-shaped DNA comprising: (A) a nucleic acid region comprising 2 to 5 arbitrary nucleotides; (B) a nucleic acid region comprising a "gna" or "gnna" base sequence, wherein each "n" represents "g", "t", "a", or "c", a base analogue, or a modified base; and (C) a nucleic acid region comprising a base sequence complementary to the nucleic acid region (A), sequentially from the 5' end toward the 3' end.
EP2614054A1 Ethyne derivatives, pharmaceutical compositions and uses thereof invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
WO2010028419A1 Prevention of psychotic disorders and/or treatment of psychotic symptoms The present invention relates to methods of preventing a psychotic disorder in a subject in need of intervention including administering to the subject a composition including EPA (eicosapentanoic acid) and DHA (docosahexaenoic acid). Methods of treating pre-psychotic symptoms in a subject, including administering to the subject a composition including EPA and DHA are also included.
US20100216737 Inactivation of miR-34a by abberant CpG methylation in cancer The present application refers to methods for cancer diagnosis and treatment, particularly in types of cancers associated with aberrant CpG methylation of the miR-34a promoter.
CN101723894A N-quinoline amide derivatives and preparation method and application thereof The invention discloses quinoline amide derivatives which are characterized by comprising the following general formula. in the general formula, when X is equal to C and R1 is equal to OH, R2 is equal to CH3, C1, BR and F or I and R3, R4, R5 and H are equal; or R3 is equal to Br, F or I, and R2, R4, R5 and H are equal; or R4 is equal to Br, F or I and R2, R3, R5 and H are equal; or R5 is equal to Cl, Br, F or I and R2, R3, R4 and H are equal; when X is equal to N, R4 is equal to CH3, R1 is equal to Cl, Br, F or I, R2, R3 and H are equal and R5 is not included; and or R1 is equal to Cl, Br, F or I, R4 is equal to OH or H, R3 is equal to H and R5 is not included. Founded by the research, the quinoline amide derivatives have strong specific bonding ability with VEGFR and the bonding of vascular endothelial growth factors in tumor cells and the VEGFR is blocked off by the bonding of the quinoline amide derivatives and the VEGFR, thereby fundamentally inhibiting the vasculogenesis and signal transduction of cancer cells and inhibiting the proliferation of the cancer cells, therefore, the quinoline amide derivatives can be applied to preparing an anti-tumor medicament. The invention also discloses the preparation method of the quinoline amide derivatives.
EP2616083A2 Removal of toxins from gastrointestinal fluids A process for the removal of toxic cations and anions from gastrointestinal fluids is disclosed. A pH-increasing medication is administered prior to or together with a microporous cation exchanger. An additional feature of the invention is the use of a proton form of the microporous cation exchanger. The acidity of the gastrointestinal fluids is decreased to improve the stability of the microporous cation exchangers, which are represented by the empirical formula: ApMxZr1-xSinGeyOm (I) or ApMxTi1-xSinGeyOm (II)
WO2005034929A3 Tissue remodeling and vascularization The present invention relates to methods, compounds, and medicaments for coordinate induction of tissue remodeling and vascularization, and for therapeutic or prophylactic treatment of disorders associated with vascular insufficiency.
CN101817829A 4-substituted anilino-podophyllotoxine derivative and application The invention provides a 4-substituted anilino-podophyllotoxine derivative which refers to a 4'-O-demethyl-4-deoxy-4-substituted anilino-podophyllotoxine derivative. A series of compounds with anti-cancer activity is synthetized by taking the traditional drug etoposide as a lead compound by structural transformation; primary in vitro screening and in vivo antitumor tests show that the compounds have better anti-tumor activity, wherein when the compound GL3 improves the anti-tumor action, the toxicity of the compound GL3 is obviously reduced, and thereby, the compound GL3 can be used for preparing anti-tumor drugs which has higher antitumor activity and lower toxicity and has effect on multi-drug drug resistant tumors. The structural general formula of the 4-substituted anilino-podophyllotoxine derivative is shown in the specification.
US20100120891 Use of a galectin-1-targeted rnai-based approach for the treatment of cancer The present invention relates to an RNAi molecule suitable for reducing the expression of galectin-1 containing any of the sequences of SEQ ID NOs: 1-33, and preferably the sequences of SEQ ID NO: 2, 3, or 4, and to the use thereof as a medicament, or for the manufacture of a medicament for treating and/or for delaying the progression of cancer, preferably glioma, pancreatic cancer, head and neck cancer, melanoma, non-small-cell lung cancer and non-Hodgkin's lymphoma. The present invention also relates to compositions and methods for treating and for delaying the progression of cancer, preferably glioma, pancreatic cancer, head and neck cancer, melanoma, non-small-cell lung cancer and non-Hodgkin's lymphoma, for reducing the migration of tumor cells, preferably cells of glioma, pancreatic cancer, head and neck cancer, melanoma, non-small-cell lung cancer and non-Hodgkin's lymphoma, and/or for enhancing the efficacy of cancer therapies for the treatment of cancer, preferably glioma, pancreatic cancer, head and neck cancer, melanoma, non-small-cell lung cancer and non-Hodgkin's lymphoma, selected from the group comprising chemotherapy, radiation therapy, immunotherapy, and/or gene therapy.
US20100137363 Substituted Indoles And Methods Of Their Use The present invention relates generally to substituted indoles and methods of using them.
US20070092567 Stable controlled release pharmaceutical compositions containing fenofibrate and pravastatin A controlled Release Pharmaceutical composition comprising an effective amount of Pravastatin and Fenofibrate, characterised in that the difference, in absolute value, between the times of maximal concentration (Tmax) of Pravastatin and Fenofibric acid is not less than 1.5 hours upon administration with food to humans.
CN101259119B Application of serine protease inhibitor and its derivative in fertility regulation The invention provides a reversible embryo implantation inhibitor, i.e. 4-(2-aminoethyl) benzenesulfonyl fluoride (AEBSF) and live derivatives or pharmaceutically acceptable salts thereof. The invention also discloses the application of live derivatives or pharmaceutically acceptable salts of AEBSF in preparing compositions used for inhibiting the implantation of embryos.
CN101926822A Use of silicon dioxide mesoporous material in preparation of antidote for treating heavy metal poisoning The invention discloses the use of a silicon dioxide mesoporous material in the preparation of an antidote for treating heavy metal poisoning, and provides the use of a new medicament for stopping enterohepatic circulation for treating heavy metal poisoning. The silicon dioxide material has a mesoporous structure; the internal and external surfaces of the mesopores are modified and connected with functional groups having sulfydryls; and the silicon dioxide mesoporous material is prepared into the antidote for absorbing heavy metals in the gastrointestinal tract.
CN101250212A 20(S) or 20(R)-dammarane-3 beta,12 beta, 20,25-tetraalcohol derivative, its salt and use thereof The invention provides a 20(S)/20(R)-dammarane-3beta, 12beta, 20, 25-tetraol derivative, relative salt and anti-tumor application, belonging to medical technical field, wherein the 20(S)/20(R)-dammarane-3beta, 12beta, 20, 25-tetraol derivative and relative salt are respresented as below, the 20(S)/20(R)-dammarane-3beta, 12beta, 20, 25-tetraol derivative and relative salt can be combined with medical acceptable carrier into drug compound, to prepare anti-virus and anti-tumor drugs. The 20(S)/20(R)-dammarane-3beta, 12beta, 20, 25-tetraol derivative and relative salt have stronger anti-viruse and anti-tumor activity than dammarane-3beta, 12beta, 20, 25-tetraol, which can improve the activity of other anti-virus and anti-tumor drugs and reduce the toxicity.
US20080193454 Identification of Surface-Associated Antigens for Tumor Diagnosis and Therapy The invention relates to the identification of gene products that are the result of tumor-associated expression and the nucleic acids encoding the same. The invention also relates to the therapy and diagnosis of diseases wherein these gene products are the result of an aberrant tumor-associated expression. The invention also relates to the proteins, polypeptides and peptides that are the result of tumor-associated expression and to the nucleic acids encoding the same.
EP2527351A1 Lipophosphonoxins, method of their preparation and use The invention discloses lipophosphonoxins of general formula I, wherein R1 is (C8-C22)alkyl or hexadecyloxypropyl, tetradecyloxypropyl, tetradecyloxyethyl or hexadecyloxyethyl and R2 is uracil, thymin or cytosin, R3 is selected from group comprising compounds of general formula II and III, where R4 is H or CH2OH, R5 is H or OH, R6 is H or OH, R7 is H or CH2OH, R8 is H or CH2OH, R9 is H or OH, R10 is H or OH, R11 is H or OH, R12 is H or CH2OH. Described are also diastereomers and mixtures of diastereomers of compounds of general formula I as well as corresponding pharmaceutically acceptable salts and hydrates and also a suitable method of preparation of such compounds. All described compounds of general formula I can be used as antibacterial agents or as active components of disinfectants and/or of selective in vitro growth media.
WO2008134844A1 Branched-chain amino acid composition for improving skeletal muscle protein metabolism The present invention relates to compositions and methods for improving skeletal muscle protein metabolism through encouraging skeletal muscle protein synthesis, reducing skeletal muscle protein degradation, and attenuating inflammatory signalling in exercising muscle. The compositions of the present invention comprise branched-chain amino acids, a plant extract that attenuates NF-ϰB activity and γ-butyrobetaine, and optionally, ethyl pyruvate or diferuloylmethane.
CN1895240A Medicine-releasing system of compound amithiourea preparation A medicine releasing system for the compound antib is prepared through preparing the micropills, microtablets, or particles of antib, coating, proportionally mixing with retozide, and filling the mixture in capsules. It can prevent the antib from being degradaged by gastric acid.
US20100233690 Use of genes identified to be involved in tumor development for the development of anti-cancer drugs and diagnosis of cancer The invention relates to the use of inhibitors of the expressed proteins of the murine genes and/or their human homologues listed in Table 1 for the preparation of a therapeutical composition for the treatment of cancer, in particular for the treatment of solid tumors of lung, colon, breast, prostate, ovarian, pancreas and leukemia and the use of the genes listed in Table 1 for the diagnosis of cancer. The invention also relates to the therapeutical compositions comprising the inhibitors and to methods for development of the inhibitor compounds.
CN103705508A 2-[1-(1,2,4-triazole-1-yl) butyl-2-methylene aminoxy] acethydrazide and medical application thereof The invention relates to 2-[1-(1,2,4-triazole-1-yl) butyl-2-methylene aminoxy] acethydrazide shown as a chemical structural formula I or application of isomers thereof in preparation of fluenza virus neuraminidase inhibitors. According to the structural formula I, R and R1 are selected from hydrogen, C1-C2 alkyl, C3-C4 straight chain or branched chain alkyl; in the formula, X1 and X5 are selected from H, methyl, ethyl, hydroxyl, methoxy, ethoxy, fluorine, chlorine, bromine, iodine or nitro; X2 and X4 are selected from hydrogen, C1-C2 alkyl, C3-C4 straight chain or branched chain alkyl, hydroxyl, methoxy, ethoxy, fluorine, chlorine, bromine, iodine or nitro; X3 is selected from H, methyl, ethyl, hydroxyl, methoxy, ethoxy, fluorine, chlorine, bromine, iodine, nitro, dimethylamino, trifluoromethyl or trifluoromethoxy.
WO2007037550A9 Therapeutic or diagnostic application of tsta3 gene It is intended to provide a therapeutic agent for cancer containing an expression inhibitor or activity inhibitor of TSTA3 protein; a method for screening a compound which can be used as an active ingredient of such a therapeutic agent; an antibody against the TSTA3 protein; a diagnostic agent for cancer/a diagnostic method for cancer using the antibody and the like.
CN101906006A Method for efficiently synthesizing cis-stilbene derivative and phosphate disodium salt predrug thereof The invention discloses a preparation method of a compound shown in the formula II. The method comprises the following steps: (a) under the irradiation of 254nm of ultraviolet light, performing a Wittig reaction to obtain the compound shown in the formula II, wherein R represents CH3, C2H5, C3H7, CH2F, CHF2, CF3, CH2CF3, CF2CF3 or CF2CH3; and Rp represents Si(CH3)2t-Bu, C(C6H5)3, (CH3)3COCO or trityl resin. Further, the invention also discloses a preparation method of a phosphate disodium salt predrug of high-purity cis-stilbene derivative; and the method comprises the following steps: using oxygen to oxidize tetrabenzyl pyrophosphate or 2-chloro-1,3,2-dioxaphospholane and perform the phosphate esterification reaction, and using trimethylbromosilane and sodium methoxide to perform basic hydrolysis.
WO2007112574A1 Extended release composition of venlafaxine An extended release composition that comprises a coated compressed core. The coated compressed core has a core and a coating composition. The compressed core comprises at least about 45 wt% of a venlafaxine ingredient; less than about 50 wt% of at least one component that acts as both a diluent and a compression aid; less than about 10 wt% of at least one glidant; and less than about 10 wt% of at least one lubricant. The coating composition comprises at least one water soluble gellable polymer; and at least one water insoluble organosoluble polymer.
US20120283270 Extracts and beverages containing 2,5-piperazinedione,3,6-bis(phenylmethyl)-, (3s,6s)- The present invention aims to provide extracts or beverages containing 2,5-piperazinedione,3,6-bis(phenylmethyl)-,(3S,6S)—, which is a useful substance with an improving effect on learning motivation, in an easy-to-ingest form and at a high concentration. Extracts or beverages whose ratio between the content of 2,5-piperazinedione,3,6-bis(phenyl-methyl)-,(3S,6S)— (unit: μg/100 g) and Brix(Bx) is 6 (μg/100 g)/Bx or more can be ingested continuously over a long period of time as foods and beverages useful for improvement of learning motivation.
US20110076326 Modified protein excipient for delayed-release tablet The present invention relates to delayed release oral formulations comprising active ingredients and modified proteins used as excipients. The proteins have chemical modifications such as succmylation, deammation, glytarylation or phosphorylation which decrease the isoelectric point of the protein compared to the protein's native isoelectric point and enhance protem-protem interactions, thereby reducing solubility and swelling, and delaying release of the active ingredient when the formulation is ingested orally. Particularly, the invention relates to tablets that comprise an excipient of chemically-modified food proteins such as soy proteins or -lactoglobulm useful for delaying release of an active ingredient such as a pharmaceutical drug or a probiotic.
CN102247381A VitaminD2-and-vitaminE-containing medicinal composition for injection and preparation method thereof The invention discloses a vitaminD2-and-vitaminE-containing medicinal composition for injection and a preparation method thereof. The vitaminD2-and-vitaminE-containing medicinal composition comprises the following raw materials in weight by weight: 25 to 20 parts of vitamin D, 0.1 to 3 parts of vitamin E, and a proper amount of oil for injection. The preparation method comprises the following steps: 1, selecting a brown glass ampoule bottle; 2, disinfecting the processing area and equipment; 3, sterilizing a pot, a stainless steel pump and a liquid tube, which are used for preparing materials; 4, adding active carbon into the oil for injection for later use; 5, adding vitamin D2 and vitamin E into the pot, and after the vitamin D2 and vitamin E dissolves, opening the stainless steel pump, mixing and obtaining vitamin medicinal composition liquid; 6, filtering the vitamin medicinal composition liquid to obtain a finely filtered vitamin medicinal composition; and 7, filling the finely filtered vitamin medicinal composition into the brown glass ampoule bottle. The medicinal composition is used for treating patients who suffer from senile osteoporosis and hepatic diseases, need medicines for a long time and are incapable of taking vitamin D2 and vitamin E orally, and the effectiveness of the medicinal composition is quick and the utilization degree is high.
US20130072531 Solid dispersion comprising an anti-hiv agent The present invention relates to solid dispersions comprising a compound of formula or a salt, a solvate or a solvate of a salt thereof, dispersed in a polymeric, inert, non-toxic, pharmaceutically acceptable excipient.
WO2011007801A1 Anti-cancer agent, method for inducing apoptosis of cancer cells, and method for screening for anti-cancer agent Disclosed is an anti-cancer agent which can inhibit the progression of cell cycle in the M phase, unlike taxane anti-cancer agents. The anti-cancer agent comprises a compound capable of inhibiting specifically the expression and/or function of RBM8A depicted in SEQ ID NO:1, Magoh depicted in SEQ ID NO:3 or an isoform thereof. The anti-cancer agent can inhibit the expression and/or function of RBM8A or Magoh in cancer cells to terminate the cell cycle in the M phase, thereby inhibiting the proliferation of the cells. Therefore, the anti-cancer agent can inhibit the proliferation of cancer cells and induce the apoptosis of cancer cells, leading to the cure of cancer.
EP1824498A2 Methods and compositions for treating cellular proliferative diseases The present invention relates to compounds and pharmaceutical compositions for treating cellular proliferative disorders, screening assays for identifying such compounds, and methods for treating such disorders.
CN103432110A Application of salvianolic acid A freeze-dried injection in preparing drug for rescuing ischemic penumbra The invention relates to an application of a salvianolic acid A freeze-dried injection in preparing a drug for rescuing ischemic penumbra. The salvianolic acid A freeze-dried injection comprises a salvianolic acid A-containing main raw material, a filling agent and an antioxidant. The freeze-dried injection is prepared by the following components by weight: 20 g-60 g of the salvianolic acid A-containing main raw material, 20 g-60 g of the filling agent and the antioxidant accounting for 0.02%-0.1% of a total weight. The salvianolic acid A-containing main raw material comprises 94%-97% of salvianolic acid A, 0.2%-1.5% of alkannic acid, 0.2%-1.5% of rosmarinic acid, 0.2%-1.5% of salvianolic acid B and 0.4%-2.0% of salvianolic acid C.
US20110065761 Methods of treating nerve-related vision disorders This invention provides reagents and methods for delivering insulin, insulinomimetic agents, and the like to a vertebrate eye via subconjunctival routes, sub-Tenon's routes, or intravitreal routes for treatment of nerve-related vision disorders such as diabetic retinopathy, and formulations useful in the practice of the disclosed methods
US20050197314 Synergistic combination of immunostimulatory CpG oligonucleotides and the immunopotentiating cytokine Flt3 ligand; immunotherapy of tumors, viral infections; cancer vaccines The present invention relates to synergistic combinations of immunostimulatory CpG oligonucleotides and immunopotentiating cytokines. In particular, the invention relates to methods of stimulating an immune response using the synergistic combination of compounds and products related thereto.
WO2013142281A1 Inhibition of mcl-1 and/or bfl-1/a1 This disclosure features compounds and pharmaceutically acceptable salts thereof that inhibit MCL-1 and/or BFL-1/A1 and compositions containing the same. This disclosure also features combinations that include one or more of the MCL-1/BFL-1/A1 inhibitor compounds described herein, or a pharmaceutically acceptable salt thereof; and one or more additional therapeutic agents (e.g., one or more chemotherapeutic agents (including small molecule and/or anti-body based chemotherapy and/or radiation); e.g., one or more therapeutic agents that modulate apoptosis; e.g., one or more therapeutic agents that bind to and inhibit anti-apoptotic proteins or modulate them indirectly; e.g., one or more therapeutic agents that bind to and inhibit, or indirectly modulate, anti-apoptotic BCL-2, BCL-XL, BCL-w, MCL-1, and/or BFL-1/A1; e.g., one or more therapeutic agents that directly bind to and inhibit anti-apoptotic BCL-2 / BCL-XL; e.g., agents such as ABT-199, ABT-263 and ABT-737; e.g., ABT-737), or (where applicable) a pharmaceutically acceptable salt of the one or more therapeutic agents (as well as compositions containing the same). Also featured are methods of using such compounds, salts, combinations, and compositions, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., diseased or damaged cells; e.g., insufficient apoptosis of diseased or damaged cells or reduced apoptosis of diseased or damaged cells)..
EP1431275B1 Diaryl ether derivative, addition salt thereof, and immunosuppressant A diaryl ether derivative having excellent immunosuppressive activity and reduced in side effects. The diaryl ether derivative is represented by the general formula (1): (1) {e.g., 2-amino-2-[4-(3-benzyloxyphenoxy)-2-chlorophenyl]propyl-1,3-propanediol}.
US20110130443 Compositions And Methods For Inhibiting Expression Of Factor V Leiden Mutant Gene The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of the Factor V Leiden mutant gene (Factor V Leiden mutant gene), comprising an antisense strand having a nucleotide sequence which is less that 25 nucleotides in length and which is substantially complementary to at least a part of the Factor V Leiden mutant gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of the Factor V Leiden mutant gene using the pharmaceutical composition; and methods for inhibiting the expression of the Factor V Leiden mutant gene in a cell.
CN101152174A Stable rifamycin sodium injection prescription and preparing method of the same The invention discloses a rifamycin sodium injection and a freeze-dried injection formula and the preparation method. The preparation process is simple and the products greatly improve the stability of rafamycin sodium, stabilize and control the quality. The injection contains C37H47NO12 proportion of rifamycin sodium, 1.0 to 2.0 proportion of organic solvent for injection, 0.008 to 0.016 proportion of antioxidant, proper amount of pH regulator to regulate the pH value to between 5.0 to 7.5, and the allowance is water for injection. The freeze-dried injection contains C37H47NO12 proportion of rifamycin sodium, 20220 to 0.16 proportion of antioxidant, 0.12 proportion of mannitol, proper amount of regulator to regulate the pH value to between 5.0 to 7.5. Formula dosage of antioxidant is added with water for injection to dissolve, added with organic solvent for injection, added with C37H47NO12 proportion of rifamycin sodium, and the pH value is regulated to between 5.0 to 7.0. And then the formula dosage is added with activated carbon for injection with an amount of 0.1 percent of the solution, and is stirred for 10 minutes, filtered and decarbonized through 0.2 Mu m microporous membrane, replenished with water for injection to total content, bottled in 1 to 20ml brown bottle biocare, aerated with nitrogen and sealed. Then the dosage is sterilized in 100 temperature vapor, cooled, tested and packaged to produce finished product.
CN103405411A Applications of Chukrasone B in medicaments for treating leukemia The invention discloses applications of Chukrasone B in preparing medicaments for treating leukemia, which belong to the field of medicines. The invention discloses the application of Chukrasone B in preparing medicaments for treating leukemia, the application of Chukrasone B in preparing medicaments for inhibiting the proliferation of leukemia cells, and the application of Chukrasone B in preparing medicaments for inducing the apoptosis of leukemia cells. The Chukrasone B is used for treating leukemia through inhibiting the proliferation of leukemia cells and inducing the apoptosis of leukemia cells. The application of Chukrasone B in preparing medicaments for treating leukemia provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone B belongs to a brand-new skeleton type, the Chukrasone B has an unexpectedly strong inhibitory activity to leukemia cells.
WO2010005572A3 Alpha-keto heterocycles as faah inhibitors The invention provides a series of -αketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof.
CN1568989A Dripping pill of loperamide hydrochloride and its preparation method The invention relates to an Loperamide Hydrochloride drop pill prepared by utilizing ultramicro disintegration and drop pill manufacturing process, which has the advantages of improving collapse and dissolving speed, dissolving out speed and degree, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use. It has good compliance, thus is especially suitable for children, the elderly, bedridden patients and dysphagia patients.
US7547690 Compounds for the treatment of Hepatitis C The invention encompasses compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
US20100305130 Nasal spray device and method of use thereof A single-use sprayer for nasal anesthesia is disclosed. The single-use sprayer includes a single dose of anesthetic and a delivery system adapted to dispense the single dose of anesthetic into a nostril. The single-use sprayer prevents patient-to-patient contamination, is easy to use and allows for self-administration, and has a simple, disposable configuration so as to lower the production cost.
CA2804210A1 Methods and compositions for the specific inhibition of androgen receptor by double-stranded rna This invention relates to compounds, compositions, and methods useful for reducing AR target RNA and protein levels via use of dsRNAs, e.g., Dicer substrate siRNA (DsiRNA) agents.
EP1226148B1 Novel oligosaccharides, preparation method and pharmaceutical compositions containing same The invention concerns oligosaccharides of formula (I), their mixtures, their diastereomers, methods for preparing them and pharmaceutical compositions containing them.
CN103012621A High-purity heparin benzyl ester salt and preparation method and application thereof The invention relates to high-purity heparin benzyl ester salt and a preparation method and application thereof. Specifically, the heparin benzyl ester salt is prepared by subjecting heparin benzyl ester salt containing quaternary ammonium salt to react with an aqueous solution of alkali metal or alkaline-earth metal salt, then adding a solvent in which heparin benzyl ester metal salt or alkaline-earth metal salt is insoluble and carrying out precipitation separation. The heparin benzyl ester salt and the preparation method have the characteristics that the heparin benzyl ester salt has high purity and especially has few quaternary ammonium salt residues; the preparation method is simple, achieves industrial production easily and can be used for preparing high-purity low molecular heparin; and the yield is high.
WO2012025237A9 Substituted 2-amino-quinoline-3-carboxamides as kcnq2/3 modulators The invention relates to substituted 2-amino-quinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
US6867208 Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
EP2782581A1 Electrolyte purgatives The invention provides compositions for use in purgatives, for use as purgatives, and to methods for inducing purgation of the colon. In alternative embodiments, the invention provides compositions, e.g., a purgative, comprising: a water-soluble sodium salt (especially sodium sulphate), a water-soluble potassium salt (especially potassium sulphate), and a water-soluble magnesium salt (especially magnesium sulphate); and, compositions further comprising: a bisoxatin, or a detergent stool softening agent (such as sodium picosulphate) and/or a water-soluble sugar (such as xylose or equivalent); or, compositions having these ingredients at different amounts, but at equivalent proportions. In alternative embodiments, the invention provides purgative compositions comprising electrolytes, salts, sugars, bisoxatin, dyes and biofilm disruptors.
US20090076068 Imidazopyridin-2-one derivatives as inhibitors of lipases and phospholipases The present invention relates to imidazopyridin-2-one derivatives of the formula I with the definitions specified in the description, to their pharmaceutically usable salts and to their use as medicaments.
CN102670542A Tramadol hydrochloride osmotic pump controlled release tablet The invention provides a novel single-chamber tramadol hydrochloride osmotic pump controlled release tablet preparation. A semi-permeable membrane containing ethyl cellulose (EC) and polyvidone (PVP) is coated on the surface of a medicament table core, so that the phenomenon of ageing of the semi-permeable membrane can be avoided, and medicament residues are reduced. The invention further provides a method for improving the anti-ageing performance of a single-chamber tramadol hydrochloride osmotic pump controlled release tablet. The method is characterized in that: ethyl cellulose-polyvidone is taken as a semi-permeable membrane material. Moreover, the invention further provides an application of an ethyl cellulose-polyvidone composition to preparation of a single-chamber tramadol hydrochloride osmotic pump controlled release tablet with anti-ageing performance.
US20080161419 Selective antagonistic compounds 5-HT2B and 5-HT7 receptors; reduced side effects The present invention relates to prophylactic antimigraine agents comprising as an active ingredient a dual antagonist for the 5-HT2B and 5-HT7 receptors, the antagonist having a binding affinity selective for the 5-HT2B and 5-HT7 receptors. Since these prophylactic antimigraine agents show an excellent pharmacological effect in comparison with the cases in which a 5-HT2B receptor antagonist having a selective binding affinity to the 5-HT2B receptor or a 5-HT7 receptor antagonist having a selective binding affinity to the 5-HT7 receptor is used alone, they are useful as drugs which are excellent in prophylaxis of migraine and in which the side effects found in the existing prophylactic antimigraine agents are reduced.
US20120115778 Methods of Suppressing Appetite by the Administration of Antagonists of the Serotonin HTR1a or HTR2b Receptors or Inhibitors of TPH2 Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.
CN102824422A Pharmaceutical composition containing total glucosides of paeony and pentoxifylline and application of pharmaceutical composition The invention discloses a pharmaceutical composition containing total glucosides of paeony and pentoxifylline. The weight ratio of the total glucosides of paeony to the pentoxifylline is (5-20):1. The pharmaceutical composition is remarkable in curative effect in the aspect of anti-inflammatory immunity and is especially suitable for treating rheumatoid arthritis.
WO2007008016A1 A compound comprising prodigiosin isolated from serratia marcescence b-1231 kctc 0386bp for provention and treatment of acute graft-versus-host disease This invention relates to a composition for the prevention and treatment of acute graft-versus-host disease comprising prodigiosin isolated from Serratia marcescence B- 1231 KCTC 0386BP, as an effective ingredient. The prodigiosin is immunosuppressive by selectively suppressing the proliferation of T-cells through the suppression of the expression of IL-2 receptors, which is needed for the activation of T-cells. Prodigiosin can be used either alone or in conjunction with cyclosporin A for greater effect, since the two substances have different mode of actions. These make prodigiosin effective for the prevention and treatment of acute graft-versus-host disease.
WO2009011567A1 Crystalline forms of efavirenz The present invention provides a novel solid form of Efavirenz, crystalline form of Efavirenz with sodium deoxycholate, designated Efavirenz : sodium deoxycholate,, methods for the preparation of Efavirenz : sodium deoxycholate, and the use of Efavirenz: sodium deoxycholate, in pharmaceutical applications, in particular in anti- HIV medicaments. The crystalline form of Efavirenz : sodium deoxycholate, can be used in combination with other anti-HIV medicaments such as Tenofovir DF and Emtricitabine.
WO2008100769A3 Process for selective sulfation of aromatic hydroxyl groups The present invention relates to processes for selective sulfation of an aromatic hydroxyl group over an aliphatic hydroxyl group where both are present in the same molecule. This invention also relates to processes for selective sulfation of the aromatic hydroxyl group of equilin, equilenin, estradiol, estra(1,3,5-triene)- 3,16,17-triol, dihydroequilenin or dihydroequilin. This invention further relates to alkali metal salts of dihydroequilenin sulfates, dihydroequilin sulfates, estradiol sulfates, and estriol sulfates, processes for making thereof, stable compositions comprising thereof, and the use thereof.
US20120053214 The little molecule compound which used for promoting the stem cells hyperplasia and the use thereof The invention provides small molecule compounds capable of accelerating proliferation of stem cells and uses thereof. The compounds play an important role in the research of stem cell proliferation mechanism. The invention further relates to the uses of the compounds and relevant compounds thereof in the preparation of stem cell proliferation accelerators and the preparation of medicines accelerating stem cell proliferation. The invention also relates to the uses of the compounds in the preparation of medicines for the treatment of various diseases arising from functional cells loss or damage. The diseases arising from stem cell trauma comprise diseases related to the degeneration or damage of nervous system cells, blood system diseases, diseases related to the loss or damage of cardiovascular cells, skin burn and the like.
US8003628 Methods of inhibiting osteoclast activity Methods of inhibiting osteoclastogenesis and the activity of osteoclasts are disclosed. Methods of treating patients who have diseases characterized bone loss are disclosed. According to the methods, an amount of a TRANCE/RANK inhibitor effective to inhibit osteoclastogenesis is administered to the patient. Pharmaceutical compositions which comprise TRANCE/RANK inhibitor in an amount effective to inhibit osteoclastogenesis. Methods of modulating dendritic cell maturation, T cell proliferation, and/or CD40 receptor systems in an individual are disclosed. The methods comprise the step of administering to the individual an amount of a TRANCE/RANK inhibitor effective to modulating dendritic cell maturation, T cell proliferation, and/or CD40 receptor systems.
WO2006131296A1 Substituted n-benzo [d] isoxazol-3-yl-amine derivatives as inhibitors of mglur5, serotonine (5-ht) and noradrenaline receptors, and the use thereof for producing medicaments The invention relates to substituted N-benzo[d]isoxazol-3-yl-amine derivatives of formula (I) wherein R1,R2,R3,R4 and R5 are defined as in patent claim 1. The invention also relates to the use of said compounds for producing medicaments.
WO2014085367A1 Substituted benztropine analogs for treatment of dementia A method for treating a condition selected from Alzheimer's disease, mild cognitive impairment, age-associated dementia, and frontotemporal dementia, comprises administering to a patient in need of such treatment a safe and effective amount of a compound having the formula (I): wherein R is selected from hydrogen, alkyl, alkoxy, arylalkyl, aryloxyalkyl, cinnamyl and acyl; and R1 and R2 are independently selected from hydrogen, alkyl, alkoxy, hydroxy, halogen, cyano, amino and nitro; with the proviso that if R is methyl, R1 and R2 are not both hydrogen; and the compound comprises pharmaceutically acceptable salts thereof.
WO2010139252A1 Use of isothiocyanates for promoting growth of hairs The present invention provides the use of isothiocyanates for promoting growth of hairs, particularly the new use of natural or synthetic isothiocyanates or derivates, metabolites thereof for promoting growth of hairs, especially preventing and/or treating alopecia (preferably androgenetic alopecia) and the associated preventive, therapeutic and/or cosmetic methods.
CN103360385A Compound and medicament for treating MRSA (Methicillin-resistant Staphylococcus Aureus) infection The invention provides a compound and a preparation method thereof. The compound has a structure shown in a structural formula (I), wherein MRAS-expressed beta-lactamase can activate photosensitive groups in the compound provided by the invention, so as to generate active oxygen for exterminating MRAS without influencing a microbe and normal tissue which have unexpressed beta-lactamase, and therefore, the compound provided by the invention can achieve the beneficial effects of high efficiency, high specificity and less side effect, can be used as a photosensitizer for PACT treatment of MRSA infection and can provide a powerful tool for treating clinical patients with MRSA injection.
CN103356560A Application of Sarcaboside B in medicine used for treating prostate cancer The invention discloses an application of Sarcaboside B in preparation of a medicine used for treating prostate cancer and belongs to the technical field of new applications of medicines. In vitro MTT (methyl thiazolyl tetrazolium) antineoplastic activity evaluation shows that Sarcaboside B has an obvious inhibiting effect on growth of human prostate cancer cell strains such as ALVA, gpc-1, 9L-B and Du145, so that Sarcaboside B can be used for preparing an anti-prostate-cancer medicine and has a good development application prospect; the application of Sarcaboside B in preparation of the medicine used for treating prostate cancer is disclosed for the first time, a brand new skeleton type is adopted, and Sarcaboside B has an unexpected inhibitory activity on prostate cancer cells.
US20050153920 Ribozymes used as prodrugs The invention concerns prodrugs wherein the drug converts from its inactive form to its active form due to catalytic activity of nucleic acid sequences associated with the prodrug.
US20080188428 Bioinformatically detectable group of novel hiv regulatory genes and uses thereof The present invention relates to a group of novel viral RNA regulatory genes, here identified as “viral genomic address messenger genes” or “VGAM genes”, and as “viral genomic record” or “VGR genes”. VGAM genes selectively inhibit translation of known host target genes, and are believed to represent a novel pervasive viral attack mechanism. VGR genes encode an operon-like cluster of VGAM genes. VGAM and viral VGR genes may therefore be useful in diagnosing, preventing and treating viral disease. Several nucleic acid molecules are provided respectively encoding several VGAM genes, as are vectors and probes, both comprising the nucleic acid molecules, and methods and systems for detecting VGAM genes, and for counteracting their activity.
CN103054821A Ibuprofen arginine tablet and preparation method thereof The invention relates to an ibuprofen arginine tablet which comprises, by weight, 90.01 to 99.00% of ibuprofen arginine, with the balance being adjuvant. The invention further relates to a preparation method for the ibuprofen arginine tablet. In the tablet provided by the invention, the content of ibuprofen arginine is greater than 90%, and a small amount of the adjuvant is contained; the tablet has better stability and higher security; after granulation, the tablet undergoes coating, so a better taste masking effect is obtained, and an obtained granule has better fluidity and smaller hygroscopicity. The preparation method provided by the invention has the advantages of a simple process, a short production period, high efficiency, more effective conservation of production cost and suitability for large scale industrial production.
EP2055306A1 Application of a gestagen in combination with an oestrogen and one or more pharmaceutically acceptable excipients/media for lactose-free oral contraception Use of gestagen in combination with estrogen and one or more auxiliary materials/carriers for producing a pharmaceutical preparation for lactose-free oral contraception, is claimed. - ACTIVITY : Contraceptive. No biological data given. - MECHANISM OF ACTION : None given.
US7335681 Inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase; Gaucher's disease, Tay Sachs disease, Fabry's disease. Sandhoff disease or GM1 gangliosidosis Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
US20070196460 External preparation for treating skin or mucosal injury caused by viral infection An external preparation containing acetylsalicylic acid or a pharmacologically acceptable salt thereof as an active ingredient, which is used for treatment of vesicle, sore or ulcer of skin or mucosa caused by a viral infection.
CN1919297A Decoction medicine for treating obstinate headache of yin deficiency type and its preparing process Disclosed is a medicinal broth for treating cough and its preparing process, wherein the medicament is prepared from the following raw materials (by weight portion): plaster stone 40-50g, root of red rooted saliva, cordate houttuynia each 25-30g, radix adenophorae, lilyturf root, lily each 18-20g, earthworm 9-12g, Chinese ephedra 5-7g, prepared rhubarb, and licorice root each 2-4g. The invention realizes easy material availability, simplified preparation, low cost, and quick effect.
EP1265579B1 Container for linezolid intravenous solution The present invention is a container for an IV aqueous solution of a Gram-positive oxazolidinone agent, such as linezolid as the compound of formula (I) which comprises having the container-solution contact surface material being a polyolefin.
US6949548 administering a synergistic combination of levosimendan or a pharmaceutically acceptable salt thereof and a beta-adrenergic receptor antagonist to a patient in need of such treatment A combination therapy for the treatment of heart failure comprises administering a combination of levosimendan or a pharmaceutically acceptable salt thereof and a beta-adrenergic receptor antagonist to a patient. The combination synergistically reduces mortality in heart failure patients.
CN101415706A Azolopyridin-3-one derivatives as inhibitors of endothelial lipase The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings indicated in the description, their pharmaceutically usable salts and their use as medicinal substances. The compounds are inhibitors of endothelial lipase.
CA2749947A1 Methods for treating estrogen receptor positive cancer by x-box binding protein 1 inhibition Provided is a method of inhibiting proliferation of estrogen receptor alpha positive tumor cells comprising the inhibition of X-box binding protein-1 (Xbp1), including inhibiting estrogen-induced proliferation.
CN1562044A Witamin D2 calcium levulinate freeze-dried emulsion and its preparing method A freeze-dried VD2 calcium pectate cream is prepared from VD2 calcium pectate, the oil for injection, stabilizer, emulsifier, pH regulator, freeze-drying protector, antiseptic and the water for injection. Its preparing process is also disclosed.
US20140093466 Hair care compositions and methods of use Hair care compositions including from about 0.005% to about 5% apigenin; from about 0.15% to about 12% of a solubilizing agent, wherein the solubilizing agent comprises an amine functional group; and at least about 20 weight percent of an aqueous carrier, where the composition has a pH ranging from about 3 to about 10, and methods of making the same are provided. These hair care compositions can be applied to any area of the scalp or hair where healthier hair appearance is desired.
CN102971306A Pyrazolopyridines as inhibitors of the kinase LRRK2 A compound of formula la or formula lb, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; -NHR3; fused aryl-C4-7-heterocycloalkyl; - CONR4R5; -NHCOR6; -C3-7-cycloalkyl; -0-C3-7-cycloalkyl; -NR3R6; and optionally substituted -C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7- heterocycloalkyl are each optionally substituted; Q is CN, halogen, or is selected from C1-6-alkyl, C3-7-cycloalkyl, heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted with one or more substituents A; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl,C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl,, Cz-B-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7- cycloalkyl, fused aryl-C-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7- cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-heterocycloalkyl ring; each R6 is independently selected from C1-6-alkyl, C3-7 cycloalkyl, C-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted; each R7 is selected from hydrogen, optionally substituted C1-6-alkyl and C3-7-cycloalkyl; each of R8 and R9 is independently hydrogen or optionally substituted C1-6-alkyl; or R8 and R9 together with the N to which they are attached form a C4-6-heterocycloalkyl; each R10 is selected from C3-7- cycloalkyl and optionally substituted C1-6-alkyl; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6-alkyl-C3-7-cycloalkyl, C4-7-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted; A is selected from halogen, - NR4S02R5, -CN, -OR6, -NR4R5, -NR7R11, hydroxyl, -CF3, -CONR4R5, -NR4COR5, -NR7(CO)NR4R5, -N02, -C02H, -C02R6, -S02R6, -S02NR4R5, -NR4COR5 ,-NR4COOR5, 6-alkyl and -COR6. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formulae la and lb.
US20090048192 Double Strand Compositions Comprising Differentially Modified Strands for Use in Gene Modulation The present invention provides double stranded compositions wherein each strand is modified to have a motif defined by positioning of β-D-ribonucleosides and sugar modified nucleosides. More particularly, the present compositions comprise one strand having an alternating motif and another strand having a hemimer motif, a blockmer motif, a fully modified motif or a positionally modified motif. At least one of the strands has complementarity to a nucleic acid target. The compositions are useful for targeting selected nucleic acid molecules and modulating the expression of one or more genes. In preferred embodiments the compositions of the present invention hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. The present invention also provides methods for modulating gene expression.
US7825095 Methods and unit dose formulations for the inhalation administration of aminoglycoside antibiotics A patient suffering from an endobronchial infection is treated by administering to the patient for inhalation a dose of less than about 4.0 ml of a nebulized aerosol formulation comprising from about 60 to about 200 mg/ml of an aminoglycoside antibiotic, such as tobramycin, in a physiologically acceptable carrier in a time period of less than about 10 minutes. Unit dose devices for storage and delivery of the aminoglycoside antibiotic formulations are also provided.
CN102988397A Application of Houttuynoid A for preparing monoamine oxidase (MAO) inhibitor medicine The invention provides application of Houttuynoid A for preparing a monoamine oxidase (MAO) inhibitor. Compared with the original MAO inhibitor, the inhibitory activity and the selectivity on MAO-A and MAO-B of the MAO inhibitor provided by the invention are greatly increased. The application of Houttuynoid A for preparing the MAO inhibitor is disclosed for the first time; because the skeleton type belongs to a brand new skeleton type and the MAO inhibitory activity of Houttuynoid A is strong unexpectedly, the possibility that other compounds give any inspiration does not exist; Houttuynoid A has outstanding substantive characteristics; and simultaneously, Houttuynoid A has obvious progress for treating diseases related to MAO imbalance.
US20120171154 purification of multi-specific receptors Disclosed is a method for preparing a composition enriched for receptors (typically molecular impringet polymers, MIPs) that bind an agent, where said receptors each specifically bind at least two discrete sites on said agent, by subjecting a sample of receptors to a first step of affinity purification with the agent where one binding site on the agent is non-accessible for binding to the receptors and subsequently subjecting the purified receptors to at least one further step of affinity purification with the agent where a second binding site on the agent is non-accessible. Also disclosed is a method for treatment, amelioration or prophylaxis of a disease selected from the group consisting of phenylketonuria (PKU, Følling's disease), hyperphenylalaninemia (HPA), alcaptonuria (black urine disease), tyrosinemia, hypertyrosinemia, myasthenia gravis, histidinemia, urocanic aciduria, maple syrup urine disease (MSUD), isovaleric acidemia (isovaleryl-CoA dehydrogenase deficiency), homocystinuria, propionic acidemia, methylmalonic acidemia, and glutaric aciduria Type 1 (GA-I), galactosemia, comprising administering to the gastrointestinal tract of a patient in need thereof an effective amount of a composition of molecular imprinted polymers (MIPs), said composition being capable of binding a symptom provoking agent of said disease.
CN103393846A Natural medicine extract and preparation method thereof The invention relates to a natural medicine extract and a preparation method thereof. The natural medicine extract comprises a radish seed and aquilaria sinensis-decocted concentration extract, sulforaphane, an aquilaria sinensis chloroform extract and an aquilaria sinensis hexane extract according to the ratio of (2-5):(6-9):(2-5):(3-6). The composition has good curative effect on the cancer chemotherapy-induced diarrhea, and can play a synergism role in cancer chemotherapy.
EP2025341A1 Ointment for combating and treating skin diseases, and process for preparing said ointment The invention relates to an ointment for treating and curing skin diseases of human beings such as psoriasis, dermatitis, acne, herpes and fungi, consisting of a composition obtained based on ingredients such as white petrolatum, , clobetasol propionate, distilled water, rosemary honey, virgin olive oil, white precipitate mercury chloride, salicylic acid, and gentian violet. It also describes a process for preparing said ointment basically consisting of preparing a completely homogenized composition from the mentioned ingredients with the use of a stirring device for a time of about 30 minutes and maintaining the temperature at around 20°C in order to obtain the cream or ointment appearance of said composition.
WO2014160502A1 Uridine nucleoside derivatives, compositions and methods of use This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.
CN102908324A Apixaban tablet The invention discloses an Apixaban tablet, which comprises the following components in parts: 1 part of Apixaban, 10-20 parts of water-soluble carrier material, 30-60 parts of filling agent, 5-10 parts of disintegrating agent and 5-10 parts of glidant. The Apixaban tablet provided by the invention improves the deficiencies in the prior art that the extracorporeal dissolution rate and the bioavailability is low. The preparation method of the Apixaban tablet disclosed by the invention is simple to operate, has good reproducibility, and is suitable for large-scale production. The Apixaban tablet is mainly used for the anti-thrombosis purpose.
US20080221132 Multi-Functional Small Molecules as Anti-Proliferative Agents The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.
EP1725569A1 Prodrugs of piperazine and substituted piperidine antiviral agents This invention provides for prodrug Compounds (I), pharmaceutical compositions thereof, and their use in treating HIV infection. Also, this invention provides for intermediate Compounds (II) useful in making prodrug Compounds (I).
US7799794 Treatment for cardiovascular disease This invention relates to a method for treating and preventing hypertension by administering a therapeutically effective amount of an agent capable of reducing uric acid levels in a patient in need of such treatment. Additionally, the scope of the invention includes a method of treating coronary heart disease by administering a therapeutically effective amount of an agent capable of reducing uric acid levels in a patient in need of such treatment.
CN102552111A Massage ointment combination The invention relates to a health care drug, in particular to massage ointment. The massage ointment comprises the following components in percentage by weight: 0.45-0.65 percent of pyridoxine hydrochloride, 2.0-3.2 percent of calcium phosphate, 4.0-6.0 percent of glycerol, 2.0-4.0 percent of vaseline, 2.0-3.0 percent of hexadecanol, 2.0-4.0 percent of liquid paraffin, 0.2-0.3 percent of methyl p-hydroxybenzoate, 5.0-7.0 percent of glycerin monostearate, and 0.8-1.0 percent of anhydrous lanolin; and the rest is deionized water. The massage cream combination has the better treatment effects on rheumatalgia, joint inflammation, muscle soreness, movement strain, traumatic injury and the like and particularly has the optimal treatment effect on strain caused by movement.
CA2676146A1 Ligand modified poly oxo-hydroxy metal ion materials, their uses and processes for their preparation Ligand-modified poly oxo-hydroxy metal ion materials and their uses are disclosed, in particular for nutritional, medical, cosmetic or biologically related applications for example for the treatment of a deficiency related to a component of the material or for the removal of an endogenous substance capable of binding to the material. The present invention further relates to processes for preparing the materials and optimising their physicochemical properties and their medical uses.
EP1827604A1 Methods and compositions for adoptive immunotherapy In a first aspect the present invention provides a method for producing an adoptive immune response to a target cell in a subject, said method including the steps of engineering a CD4+ T cell and engineering a CD8+ T cell to express a molecule capable of binding to an antigen on the target cell, and administering an effective number of the engineered CD4+ and CD8+ T cells to the subject. According to this method the CD4+ T cell and the CD8+ T cell are obtained from the subject, engineered, and re-administered to the subject to produce the adoptive immune response Applicants have found that in adoptive transfer experiments in vivo, administration of sufficient numbers of antigen engineered CD4+ in combination with engineered CD8+ cells leads to a significantly enhanced immune response to a target cell. It is demonstrated herein that the injection of CD4+ and CD8+ T cells engineered to express a molecule capable of binding to a tumor associated antigen led to significant improvement in survival of subjects having established lung metastases, compared with transfer of unfractionated spleen-derived (largely CD8+) engineered T cells. Importantly, anti-tumor responses in the subjects correlated with persistence and localization of engineered T cells at the tumor site and in the blood and spleen. Applicants have further demonstrated herein that subjects treated with engineered CD4+ and CD8+ T cells that survived primary tumor challenge could reject a subsequent rechallenge with the same tumor. The studies disclosed herein demonstrate the therapeutic advantage in the combined transfer of antigen-specific gene-modified CD4+ and CD8+ T cells to significantly enhance T cell adoptive strategies for the treatment conditions such as cancer and infectious diseases.
CN101323623A Novel fourth generation cephalosporin, preparation and use thereof The invention relates to compounds with a structural formula as I, wherein, R represents substituted or non-substituted heteroatomic ring, aromatic ring or aralkyl; the substituent can be C1-C4 alkyl, C1-C4 alkoxy, halogen, cyano, trifluoromethyl, methylmercapto, nitryl, amido, hydroxyl, carboxyl and ester. Z<+> is randomly substituted heterocyclic group containing cations and N atoms, and n is equal to 0 to 5. The invention also relates to the salts for medical purposes of the compounds, a preparation method thereof and the application thereof in antisepsis.
CN101785838A Lung cancer treatment medicine A lung cancer treatment medicine includes the initial stage medicine and later stage medicine of the disease course; wherein, the raw materials of the initial stage includes: 15-30g of wild chrysanthemum, 13-20g of radix stemonae, 20-30g of bletilla, 20-30g of cogongrass rhizoma (monkshoodvine root-bark) , 30-50g of sculellaria barbata, 15-25g of cynanchum atratum, 20-30g of vitex, 10-20g of tendril-leaved fritillary bulb, 10-20g of thunberg fritillary, 15-20g of rhizoma pinelliae preparata, 20-30g of turtle shell,10-20g of tonkinensis and 10-20g of codonopsis ussuriensis hemsl; the raw materials of the later stage medicine include:20-30g of bletilla, 15-20g of radix ampelopsis, 20-30g of gecko, 20-30g of asparagus,15-20g of radix ophiopogonis, 20-30g of polygonatum, 15-20g of dysosma, 15-30g of indian iphigenia bulb, 20-30g of radix semiaquilegiae, 20-30g of adenophora stricta,20-30g of cortex lycii radicis,15-25g of oyster, 15-25g of gypsum, 30-50g of oldenlandia diffusa, 10-20g of momordica dioica. The lung cancer treatment medicine is used for the treatment of 250 cases, wherein 80 cases are cured, significant efficacy is shown in 162 cases and no efficacy is found in 8 cases so that the cure rate is 32%, the significant efficacy rate is 64.8%, the non-efficacy rate is 3.2% and the total efficacy rate is 96.8%.
WO2010066699A1 Uracyl cyclopropyl nucleotides Compounds of the formula (I) including any possible stereoisomers thereof, wherein: R1 is hydrogen or halo; R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is a group of formula (II) R7 is optionally substituted phenyl; naphthyl; indolyl or N-C1-C6alkyloxycarbonyl- indolyl; R8 is hydrogen, C1-C6alkyl, benzyl; R8' is hydrogen, C1-C6alkyl, benzyl; or R8 and R8' together with the carbon atom to which they are attached form C3-C7cycloalkyl; R9 is C1-C10alkyl, benzyl, or optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof. pharmaceutical formulations and the use of compounds I as HCV inhibitors.
CN102188553B Medicinal wine for oral and external administration and manufacturing method thereof The invention discloses medicinal wine for oral and external administration and a manufacturing method thereof. The raw material of the medicinal wine for oral and external administration comprises the following components in part by weight: 20 to 40 parts of fennel, 20 to 40 parts of seed of Chinese dodder, 20 to 40 parts of cissus assamica, 20 to 40 parts of oroxylum indicum, 200 to 400 parts of fructus rosae laevigatae, 40 to 60 parts of Chinese angelica, 20 to 40 parts of Ligusticum wallichii, 20 to 40 parts of bark of eucommia, 30 to 50 parts of medicinal cyathula root, 20 to 40 parts ofMorinda officinalis, 10 to 30 parts of cassia bark, 20 to 40 parts of herba epimedii, 100 to 200 parts of crystal sugar, 100 to 200 parts of brown sugar, and 10,000 to 20,000 parts of white spirit. The medicinal wine for oral and external administration can be used for treating arthritis, scapulohumeral periarthritis, rhinitis and other inflammation as well as osteoproliferation, intervertebral disc herniation, pain in waist and legs, toothache and the like. The medicinal wine has remarkable effect, diversified functions, and wide application range, and the manufacturing process is simple andeasy to implement.
DE102004030305A1 Preventing or treating neurodegenerative or dementia diseases characterized by molecular pathology of microtubuli-associated tau protein comprises administering a K252a derivative Preventing or treating neurodegenerative or dementia diseases characterized by molecular pathology of microtubuli-associated tau protein comprises administering a K252a derivative (I). Preventing or treating neurodegenerative or dementia diseases characterized by molecular pathology of microtubuli-associated tau protein comprises administering a K252a derivative (I) of formula 1 or its salt. R1COOR or CONHR; R : H, Me, Et or cyclopropyl; R2, R3H, F, Me, OH, NH2, NHMe or NMe2; and Z : (H,H) or O. Independent claims are also included for: (1) identifying inhibitors of neurofibrillar degeneration and their activity by incubating metabolically active mammalian brain section tissue with candidate compounds at various concentrations, provoking tau hyperphosphorylation with a PP2A (not defined) inhibitor, quantifying tau phosphoepitopes in the tissue or tissue extracts by immunoassay, and comparing the phosphoepitope provocation with that of untreated control tissue; (2) determining a suitable dose of an inhibitor of paired helical filament-like tau hyperphosphorylation for treating a disease characterized by neurofibrillar pathology by titrating the inhibitor in brain sections stimulated with a PP2A inhibitor to determine effective tissue concentrations and pharmacokinetically evaluating a dosage scheme to produce effective concentrations in the CNS of a subject; and (3) determining a suitable dose of an inhibitor of paired helical filament-like tau hyperphosphorylation for treating a disease characterized by neurofibrillar pathology by determining a normal level of a paired helical filament-like tau phosphoepitope in the cerebrospinal fluid of healthy control subjects of the same age group, increasing the dose of an inhibitor in a subject suffering from a form of neurofibrillar degeneration at intervals of several weeks or administering increasing doses of an inhibitor identified as above to individual subjects, immunochemically evaluating the reduction in paired helical filament-like tau phosphoepitope in the cerebrospinal fluid of the same subject immediately before the start of treatment and again after several weeks of continuous administration of the inhibitor, and comparing the level of paired helical filament-like tau phosphoepitope in cerebrospinal fluid before and after the start of treatment of a subject suffering from a form of neurofibrillar degeneration, and determining the effective dose as one that reduces the paired helical filament-like tau phosphoepitope level to the range occurring in healthy controls of the same age group. [Image] - ACTIVITY : Neuroprotective; Nootropic; Antiparkinsonian; Cerebroprotective. - MECHANISM OF ACTION : Tau hyperphosphorylation inhibitor. 9(S),12(R)-Epoxy-2,3,9,10,11,12-hexahydro-10(R)-amino-9-methyl-1-oxo- 1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10 -carboxamide had an IC50 of 200 nM for inhibiting phosphorylation of AP422, AT8, AT100 and Thr231 epitopes in rat hippocampus sections, and 400 nM for inhibiting phosphorylation of the Ser262 epitope.
US20120295879 NK1 Antagonists A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
CN103495150A Detoxification and tissue regeneration promoting foot bathing powder The invention relates to a formula of detoxification and tissue regeneration promoting foot bathing powder. The detoxification and tissue regeneration promoting foot bathing powder is composed of, by weight, 10 to 30 parts of lysimachia foenum-graecum hance, 10 to 30 parts of tuber fleeceflower stems, 10 to 30 parts of divaricate saposhnikovia roots, 10 to 30 parts of minium, 10 to 30 parts of honeysuckle, 10 to 30 parts of humulus japonicus, 10 to 30 parts of night willow herb, 10 to 20 parts of wormwood, 10 to 15 parts of ginger, 10 to 15 parts of pinellia ternate and 10 to 15 parts of Chinese prickly ash. By the adoption of the detoxification and tissue regeneration promoting foot bathing powder, the effects of disinfection and itching and fatigue relieving are achieved, the powder is used for treating carbuncle furuncle pyogenic infection, eczema, incised wound bleeding, aphtha, slight corneal opacity, burns by soup and fire and the like, and the detoxification and tissue regeneration promoting foot bathing powder further has the cold dispelling and dampness removing effect, the rheumatic pain and exterior syndrome relieving effect, the mind tranquilizing and heart nourishing effect, the detoxification and tissue regeneration promoting effect, the disinfection and itching relieving effect and the like.
EP1691807A1 Indole derivatives for the treatment of bone diseases This invention relates to a method for preventing and/or treating bone diseases which comprises administering a potentiator of TGF-beta activity such as the compound of the formula [I] or pharmaceutically acceptable salts thereof to human being or animals. wherein R1 is hydrogen, etc., R2 is optionally substituted ar(lower)alkyl or optionally substituted heterocyclic(lower)alkyl, etc., R3 is hydrogen, optionally substituted hydroxy, etc., R4 is hydrogen or lower alkyl, and X is CH or N.
WO2007102571A1 Therapeutic agent for functional brain disease [PROBLEMS] To provide an agent for prevention, treatment and/or condition progression inhibition of a functional brain disease. [MEANS FOR SOLVING PROBLEMS] Disclosed is an agent for prevention, treatment and/or condition progression inhibition of a functional brain disease, wherein the agent comprises (2R)-2-propyloctanoic acid or a salt thereof. The agent can be administered safely to a patient suffering from a functional brain disease such as depression, menopausal mood disorder, perimenopausal mood disorder, panic disorder, irritable bowel syndrome, social anxiety disorder and post-traumatic stress disorder, and shows excellent effects.
CN101785784A Compound of gold nanorods and zwitter ion molecules for photo-thermal therapy of cancer and preparation method thereof The invention discloses a compound of gold nanorods and zwitter ion molecules for photo-thermal therapy of cancer and a preparation method thereof. The zwitter ion molecules at the outer layer and the gold nanorods at the inner layer form the gold nanorods interface-modified by the zwitter ion molecules. Surface chemical modification is carried out between sulfydryl in the zwitter ion molecules and the gold nanorods so as to prepare the compound in the invention. With excellent near-infrared photo-thermal converting capability, the gold nanorods have wide prospect in the photo-thermal therapy of cancer. Covalent modification is carried out on the surfaces of zwitter ions, which reflects good stability and biocompatibility of the gold nanorods. The modified zwitter ions not only promote the gold nanorods to be swallowed by cells, but also endow the gold nanorods with good electivity in targeting cancer cells. Due to the special swallowing function of the gold nanorods, the cancer cells can be quickly and effectively killed under the excitation of near-infrared light.
CN102639142A Inhibition of endosomal toll-like receptor activation The present invention relates, in general, to pattern-recognition receptors (PRRs), including toll-like receptors (TLRs), and, in particular, to a method of inhibiting nucleic acid-induced activation of, for example, endosomal TLRs using an agent that binds to the nucleic acid ("nucleic acid binding agent"), preferably, in a manner that is independent of the nucleotide sequence, the chemistry (e.g., DNA or RNA, with or without base or sugar modifications) and/or the structure (e.g., double-stranded or single-stranded, complexed or uncomplexed with, for example protein) of the nucleic acid(s) responsible for inducing TLR activation. The invention also relates to methods of identifying nucleic acid binding agents suitable for use in such methods.
WO2007012761A8 Novel polysubstituted 1,1-pyridinyl aminocyclopropanamine derivatives, method for preparing same and pharmaceutical compositions containing same The invention concerns compounds of formula (I), wherein: n represents an integer between 1 and 6 inclusively; R1 and R2 represent a hydrogen atom a (C1-C6) alkyl or (C1-C6) arylalkyl group; R3 and R4 represent a hydrogen atom, a (C1-C6) alkyl group; R5 and R6 represent a hydrogen atom, a (C1-C6) alkyl group, halogen, hydroxy, (C1-C6) alkoxy, cyano, nitro, (C2-C6) acyl, (C1-C6) alkoxycarbonyl, (C1-C6) trihalogenoalkyl, (C1-C6) trihalogenoalkoxy or amino optionally substituted; R7 represents a hydrogen atom, a (C1-C6) alkyl group or arylalkyl. The invention is useful for preparing medicines.
DE102007017298A1 New nanoparticles containing nicotine and/or cotinine useful e.g. for cigarette weaning and to treat e.g. attention-deficit hyperactivity disorder, Parkinson's disease, Alzheimer's disease and Binswanger's disease Nanoparticle containing nicotine and/or cotinine, are new. Independent claims are included for: (1) a dispersion comprising the nanoparticle; and (2) a medicament comprising the nanoparticle or the dispersion. - ACTIVITY : Antismoking; Nootropic; Tranquilizer; Antiparkinsonian; Neuroprotective; Cerebroprotective; Vasotropic. - MECHANISM OF ACTION : None given.
WO2014057115A1 Pyrrolobenzodiazepine-anti-her2 antibody conjugates Conjugates of an antibody that binds to HER2 with PBD dimers.
CN101249107A Medicament for curing extremity tinea and psoriasis The invention provides a drug for treating tinea manuum, tinea pedis and psoriasis. The drug is made from the following materials (by weight proportions): trinitrotoluene 1.5-2.5, blister beetle poweder 0.005-0.045, salicylic acid 2-5, benzoic acid 2-5, sulfur 1.5-2.5, medical-grade ethanol 70-80, and vaseline 4.5-23. The drug is counted on basis of 100 weight proportions, and vaseline is added up to 100 weight proportions. The drug is characterized in rapid action, short treatment course and less side effects. The mechanism thereof is that the drug can inhibit the synthesis of sterols in fungal cell membranes to influence the permeability of cell membranes and inhibit the growth of fungi. The drug has the effects of nourishing blood, removing dryness and wind evils, eliminating toxic substances, removing damp evils, promoting blood circulation, and improving blood stagnation. The drug combines the advantages of Chinese and western medicines, and is mainly used to treat tinea manuum, tinea pedis and psoriasis.
US20120148495 Methods for treating nicotinic acetylcholine receptor associated diseases The present invention provides methods and compositions for treating subjects suffering from a disorder associated with a nicotinic acetylcholine receptor (nAChR), methods for treating a subject having a disorder that would benefit from an increase in neural plasticity, and methods for modulating the plasticity of the primary visual cortex in subjects by modulating the expression, stability, and/or activity of Lynx1.
EP2475648A1 Ortho substituted pyrimidine compounds as jak inhibitors The present invention relates to compounds of formula (I), wherein X1 to X3, R, R2 to R7 and AA have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
EP1680105B1 Use of glucosidase inhibitors for therapy of mucoviscidosis The invention relates to the use of glycosidase inhibitors selected from compounds of general formula (1), wherein R1 represents a CH3 group, or CH2OH, R2 represents H or an alkyl group having 1-5 carbon atoms, or R1 and R2 together form a group having formula (II), with carbon in position (a) and nitrogen of formula (I) mentioned above, for the preparation of a medicament used to treat mucovisidosis.
CN103467421A Application of radix stemonae sessilifoliae non-alkaloid extract and monomers to preparation of antitumor drug The invention belongs to a radix stemonae sessilifoliae non-alkaloid extract, a preparation method thereof and a novel application of stilbene compounds to tumor drug resistance reversion. The extract is rich in non-alkaloid components, five monomeric compounds which are all stilbene compounds can be separated from the extract, and the radix stemonae sessilifoliae non-alkaloid extract is proved by a drug resistance reversion multiple measuring experiment to have tumor drug resistance reversion activity. A result shows that the radix stemonae sessilifoliae non-alkaloid extract and the five stilbene compounds have a remarkable tumor drug resistance reversion effect and are expected to be developed into tumor drug resistance reversion drugs to be clinically applied.
CA2388163C Process for formulation of carbapenem antibiotic compositions A novel process for preparing a stabilized, lyophilized carbapenem, antibiotic formulation suitable for intravenous administration to patients in need thereof, wherein the active ingredient is of formula (II). The process entails compounding an unstable, monosodium salt carbapenem with a sodium bicarbonate solution at a temperature range of from about 0° to about 5°C while maintaining a pH between about 7.0 and about 8.0, filtering the resultant solution, bottling under sterile conditions, and lyophilizing to produce the formulation.
US7030123 Indole derivatives with vascular damaging activity The invention provides a compound of Formula (I). Wherein R1, R2, R3, R10 and R11 have the meanings given in the description. Such compounds are predicted to cause the selective destruction of tumour vasculature. They may therefore be used to inhibit and/or reverse, and/or alleviate symptoms of angiogenesis and/or any disease state associated with angiogenesis.
CN101108870A Process for preparation of nucleoside phosphoric acid ester compound and application thereof The invention provides the nucleoside phosphate compound and the preparation and application, which comprises the nucleoside 3', 5'-cyclic phosphate and the 5'-phosphodiester compound. Wherein, the 3', 5'-cyclic phosphate and the derivatives work as the novel HCV inhibitor and the structural formula is shown in the drawing (I), wherein, X equals to OH and F; R equals to H, NH4, R' 4N, R' 3NH and metals such as Na, K, Ca and Li or the structural formula in the drawing (II), R' equals to linear chain or substituted alkane or cyclane, aromatic hydrocarbon, or substituted aromatic hydrocarbon or heterocyclic aromatic hydrocarbon; the four R' and three R' in the amine are the same or different. The invention has the advantages that the nucleoside phosphate compound is used for treating the HCV or is combined with the Alpha-interferon, ribavirin or other anti-HCV drugs to treat the infection of the hepatic c virus or HCV.
US20130012475 Cosmetic and Pharmaceutical Composition Comprising N-Acetylglucosamine-6-Phosphate The present invention relates to a cosmetic or pharmaceutical composition comprising N-acetylglucosamine-6-phosphate or a salt thereof and, optionally, a compound of the vitamin A family, and also to a device containing same.
DE102009041241A1 New heteroaromatic compounds are hypoxia-inducible factor inhibitors useful to treat and/or prevent e.g. cancer or tumor diseases, heart attack, arrhythmia, stroke, psoriasis, diabetic retinopathy, rheumatoid arthritis and polycythemia Heteroaromatic compounds (I) or their salts, solvates or solvate of the salts are new. Heteroaromatic compounds of formula (I) or their salts, solvates or solvate of the salts are new. Ring A : phenyl or pyridyl ring; ring B : e.g. 1H-pyrazole group, 1H-imidazole group or 1H-pyrrole group; a : connection point with the adjacent CH 2-group; aa : connection point with the ring (D); ring D : e.g. [1,2,4]oxadiazole group or [1,3,4]oxadiazole group; aaa : connection point with the ring (B); aaaa : connection point with the ring (E); ring E : phenyl or pyridyl ring; R 1> : e.g. H, halo, CN or (1-6C)-alkyl; R 2> : e.g. H, F, Cl or CN; R 3> : CH 3, C 2H 4 or CF 3; R 4> : e.g. H, halo, CN, pentafluorothio or (1-6C)-alkyl; R 5> : F, Cl, CN, CH 3, CF 3 or OH; and n : 0-2. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) a medicament comprising (I) in combination with one or more inert, non-toxic auxiliary agent; and (2) the preparation of (I). [Image] - ACTIVITY : Antiapoptotic; Cytostatic; Cardiant; Vasotropic; Antiarrhythmic; Cerebroprotective; Antipsoriatic; Ophthalmological; Antiinflammatory; Antiarthritic; Antirheumatic; Hemostatic; Vulnerary. - MECHANISM OF ACTION : Hypoxia-inducible factor inhibitor. The ability of (I) to inhibit hypoxia-inducible factor was tested in HCT 116 cells using hypoxia-inducible factor luciferase assay. The results showed that 5-({3-[3-(4-tert.butylphenyl)-1,2,4-oxadiazol-5-yl]-5-methyl-1H-pyraz ol-1-yl}methyl)-N-methyl-pyridin-2-amine exhibited an IC 5 0 value of 0.3 nmole/l.
CN103417563A Application of aurantiamarin to preparation of medicine for treating acute and chronic bronchitis The invention discloses application of aurantiamarin to preparation of a medicine for treating acute and chronic bronchitis. The aurantiamarin has a good cough-relieving effect and not toxic or side effect and can treat acute and chronic bronchitis well. The aurantiamarin-containing medicine for treating acute and chronic bronchitis has a good cough-relieving and phlegm-reducing effect, can effectively treat diseases and symptoms such as acute and chronic bronchitis and cough accompanied by excessive phlegm, and has the characteristics of stable quality, low dose and the like.
WO2013111117A3 Diaziridines for treating neurodegenerative disorders The present invention relates to compounds of formula I, use of these compounds to treat mental and neurological disorders, especially depressions and psychoses of different etiology. The compounds provided for the treatment of mental and neurological disorders are presented by a general formula I: wherein R, R', R", Y are as defined in specification or pharmaceutically acceptable salts thereof, solvates thereof such as hydrates, and pharmaceutical compositions containing such compounds.
US20130035381 Virus-inactivating composition containing low-molecular weight compound and arginine The invention provides a virus-inactivating composition with pH of 3.8 to 5.5, containing (A) 0.02 to 0.3 M arginine and (B) a component such as 0.01 to 10 mM flavonoid, polyphenol, or ascorbic acid derivative, 0.005 to 5 mass % of an arginine derivative, and 0.1 to 2.5 mass % of an extract solution of natural product.
US20100179146 Indolinone Compounds as Kinase Inhibitors Indolinone compounds of formula (I) or (II): wherein A, R1, R2, R3, R4, R5, R6, R7, and n are defined herein. Also disclosed are methods for decreasing the activity of a protein kinase and for treating a protein kinase-related disease, such as cancer, with these compounds.
US20110098229 Compositions and methods for treating dermatological conditions Provided herein are methods of improving one or more symptoms of a dermatological condition in a patient. The methods comprise topically administering a topical composition to the patient comprising a branched chain amino acid, and an enzyme activator. Also provided are kits comprising the topical composition and optionally a topical steroid.
WO2013113669A1 Isoquinoline and naphthyridine derivatives The invention provides novel compounds having the general formula (I) wherein A, R1 and R2 are as described herein, compositions including the compounds and use of the compounds for inhibiting angiogenesis by inhibition of MAP4K4.
US20080095735 Skin-Protective Polymer For Use In Teat Care Compositions This invention relates generally to the field of antimicrobial teat care compositions. More particularly, it relates to a skin-adhering antimicrobial composition comprising a copolymer which contains methacrylic acid and 2-acrylamido-2-methyl-propane sulfonic acid (AMPS) monomeric units, the antimicrobial composition hindering the transfer of bacteria from the environment to underlying teat surfaces and orifices, and which is compatible with both mammalian tissue, including skin, and teat dip compositions.
US7288659 Acylaminothiazole derivatives, their preparation and therapeutic use The invention concerns a compound of general formula (I), wherein: X represents an oxygen or sulphur atom; R1 represents, independently of each other when n=2 or 3, a halogen atom, a hydroxy, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, a trifluoromethyloxy or a methylenedioxy; R2 represents a C1-C6 alkyl group optionally substituted, a C3-C7 cycloalkyl, piperidinyl or phenyl group, the C3-C7 cycloalkyl, piperidinyl or phenyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-C6 alkyl group optionally substituted; R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 and R5′ represent, independently of each other, a hydrogen atom, a hydroxy, a halogen atom, a C1-C3 alkyl group, or R5 and R5′ form together an oxo group; R6 represents a hydrogen atom, a halogen atom, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, or a trifluoromethoxy; in the form of a base, addition to an acid, hydrate or solvate. The invention is applicable in therapy
US20110293595 Prophylactic and therapeutic treatment of Alzheimer's Disease, neuro-degenerative diseases, protein aggregation diseases, Parkinson's Disease and amyloid diseases, using phytic acid and phytate A composition and method for the treatment of Alzheimer's Disease, and/or related protein aggregation diseases and/or amyloidoses and/or a neuro-degenerative disease, and/or Parkinson's Disease and/or Parkinsonism including an effective amount of a compound selected from the group consisting of phytic acid (inositol hexakisphosphate), a phytate salt, an isomer or hydrolysate of phytic acid or a phytate salt, or a mixture of any combination thereof, being administered to a person in an amount from about 0.5 grams to about 18.75 grams at least once a week up to once per day, with or without a dephosphorylating enzyme. The dosage may be proportionately or disproportionately divided so that the dosage is administered in proportionally or disproportionately reduced amounts which cumulatively add up to a predetermined dosage, in a time period where the proportionately or disproportionately divided dosages are cumulatively equivalent in quantity to the dosage.
WO2008136748A1 Tumour growth inhibitory compounds and methods of their use Specific CpG oligonucleotide sequences, when given subcutaneously and in particular when administered on a mucous membrane, e.g. intranasally, intravaginally, or rectally, have a profound effect on various human cancer forms as confirmed in vivo, in animal studies, and in vitro, in human PBMCs collected from blood from healthy subjects and from patients suffering from CLL or FL. The compounds are also preferably used in combination with a cancer therapy chosen among radiation treatment, hormone treatment, surgical intervention, chemotherapy, immunological therapies, photodynamic therapy, laser therapy, hyperthermia, cryotherapy, angiogenesis inhibition, or a combination of any of these, and is most preferably an immunological treatment and comprises the administration of an antibody to the patient.
WO2009150462A1 Tricyclic 2,4-diamin0-l,3,5-triazine derivatives useful for the treatment of cancer and myeloproliferative disorders The present invention relates to compounds of Formula (I): (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.
CN101380299A Sustained-release injection containing methotrexate and synergist thereof A slow release injection containing amethopterin is composed of slow release microspheres and a dissolvant, wherein, the slow release microspheres comprise anticancer active components and a slow release adjuvant, and the dissolvant is a common dissolvant or a special dissolvant containing a suspending agent. The anticancer active component is a combination of amethopterin and amethopterin synergist which is selected from platinum compounds, a topoisomerase inhibitor and/or tetrazine compounds; the slow release adjuvant is selected from one or a combination of: polylactic acid, copolymer of polyglycolic acid and hydroxyacetic acid, copolymer of ethylene vinyl acetate, polifeprosan, and copolymer of FAD and sebacic acid; the suspending agent is selected from sodium carboxymethyl cellulose, and the like, and is used for suspending the anticancer active component or the slow release particles or microspheres containing the anticancer active component so as to make the slow release injection. The slow release injection is injected into tumors, which can reduce general toxic reaction of the injection, selectively improve the local drug concentration in the tumors, and enhance the curative effects of non-operative therapies such as radiotherapy, chemotherapy, and the like.
WO2014118796A1 An in-situ process for the preparation of highly pure montelukast sodium The present invention disclosed herein is a cost effective, in-situ process for the preparation of montelukast or its pharmaceutically acceptable salts of formula (1) by reacting optically pure (S)-1-{3-[2-(7-chloroquinolin-2-yl)ethylene]-phenyl}-3-[2-(1-hydroxy-1-methyl ethyl) phenyl]-propan-I-ol with methane sulfonyl chloride to afford mesylate derivative of formula (2) substantially free of impurities; followed by insitu condensing the same with disodium salt of mercapto-cyclopropyl acetic acid of formula (3) to afford montelukast free acid in good yield and purity, then converting the montelukast free acid into its substituted amine salt of formula (4). Further the montelukast substituted amine is converted into its pharmaceutically acceptable salt.
CN1919874B Antibody molecule ATF-Fc fusion albumen of antiurokinase type fibrinolysin activator receptor and use thereof The invention discloses an antibody molecule ATF-Fc merge protein and application of antiurokinase type profibrinolytic activator acceptor in biological medicine area. which is characterized by the following: the ATF-Fc merge protein is ATF area of uPA and Fc of human immune globulin IgG1; heavy chain constants region 2 and heavy chain constants region 3 through Ser-Gly-Ser-Gly-Ser joint form to dimer merge protein; possessing 742 amino acids; single-chain possesses amino acids sequence of sequence table SEQ ID No.1, wherein the front 20 amino acids is uPA signal peptide.
US7947692 Substituted thiazolo[5,4-d]pyrimidine urea derivatives There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.
CN102451168A Preparation method of naringenin tablet The invention provides a preparation method of a naringenin tablet and a tablet prepared by using the preparation method. The preparation method comprises the following steps: (1) performing salification reaction on naringenin and an alkaline compound in solvent; (2) granulating the product prepared in the step (1); and (3) mixing the particles prepared in the step (2) with other medicinal auxiliary materials, and then pressing into tablets. The prepared tablets can be used for improving the in-vitro dissolution and bioavailability of naringenin.
EP1208097B1 Substituted oxoazaheterocyclyl compounds This invention is directed to oxoazaheterocyclyl compounds which inhibit Factor Xa, to oxoazaheterocyclyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa.
WO2012169541A1 Trpv3 activator Provided are a TRPV3 activator for imparting heat sensitivity to a cosmetic material, pharmaceutical product, or oral composition, and a heat sensitivity imparting method using the same. A TRPV3 activator in which the active ingredient is an alkylphenol derivative represented by formula (A1) or (B1) [in formula (A1), R represents a hydrogen atom, a C1-4 alkyl group, or a C2-4 alkenyl group; in formula (B1), R1 represents the group -CH(CH3)CH2CH2CH=C(CH3)2 or the group -CH(CH3)CH2CH2CH2CH(CH3)2].
CN103705617A Liquid medicine for treating beriberi The invention relates to a liquid medicine for treating beriberi. The liquid medicine is prepared from the following raw materials in parts by weight: 6-9 parts of golden cypress, 6-9 parts of rhubarb, 6-9 parts of broom cypress fruit, 6-9 parts of common cnidium fruit, 6-9 parts of golden larch bark, 3-6 parts of camphor, 6-9 parts of wild pepper, 500 parts of 12-13 degrees white vinegar and 6-9 parts of 1.3-2% phenol, wherein the optimal weight part ratio of the golden cypress to the rhubarb to the broom cypress fruit to the common cnidium fruit to the golden larch bark to the camphor to the wild pepper to the white vinegar to the phenol in the medicine is 5:5:5:5:5:3:5:500:5. A preparation method of the liquid medicine comprises the following steps: weighing the golden cypress, the rhubarb, the broom cypress fruit, the common cnidium fruit, the golden larch bark, the camphor and the wild pepper in the weight parts, soaking in the white vinegar for 6 days, taking the soaked materials out, filtering the remaining leach liquor to obtain filter liquor for later use, weighing the phenol in the weight part, adding into the filter liquor, heating to 65 DEG C, stopping heating, cooling to room temperature and separately packaging the liquor to obtain finished products of the liquid medicine for treating the beriberi. The liquid medicine is applied to affected parts when in use.
WO2014085600A1 Neuroprotective agents for treatment of neurodegenerative diseases A compound having formula I is useful for treating a neurodegenerative disease: I, R1 is an C1-12 organyl group; is a C1-12 heterocyclic ring system containing 5 to 12 ring atoms and up to three heteroatoms individually selected from the group consisting of N, O, S, and Se; R2 are C1-12 organyl groups; R7, R8 are each independently, hydrogen (H), hydroxyl, oxo (i.e., carbonyl), C1-8 alkyl, C1-8 alkoxyl, C2-8 alkenyl, C2-10 alkynyl, C5-7 cycloalkyl, C5-7 cycloalkenyl, halo, C1-4 aldehyde, or -NR4 q where R4 is H, C1-8 alkyl, C2-8 alkenyl, C4-8 cycloalkyl, C4-8 cycloalkenyl, or C6-10 aryl; o is 0, 1, 2, 3, or 4; A is a C6-12 aryl group, C5-12 heteroaryl group, or an optionally substituted 3-hydroxypyridin- 4(1H)-one; p is an integer from 1 to 6; and Zm is absent or a divalent linking moiety; and m is an integer representing the number of time Z is repeated.
WO2013066134A3 Novel cinnamyl-rhodanine derivatives and pharmaceutical composition comprising same as active ingredients The present invention relates to cinnamyl-rhodanine derivative compounds or pharmaceutically acceptable salts thereof, and to a pharmaceutical composition comprising the compounds as active ingredients. More particularly, cinnamyl-rhodanine derivative compounds of the present invention inhibit the migration of cancer cells through an inhibition of activity of protein phosphatase (PPase) of PRL-3(phosphatase of regenerating liver), and therefore, can be valuably used in preventing or treating metastasis of cancer. Further, cinnamyl-rhodanine derivative compounds of the present invention inhibit the migration of vascular endothelial cells and thus inhibit angiogenesis by the same mechanism, and therefore, can be valuably used in preventing or treating angiogenesis-related diseases caused by anticancer drug or abnormal angiogenesis.
US8293283 Methods for treating oral cavity infections with chlorine dioxide Methods, devices, compositions, and systems for the alleviation of oral tissue infections by administration of chlorine dioxide are provided.
CN103339109A Tetrahydroisoquinoline derivative To provide an exceptional agent for preventing or treating dementia and schizophrenia, the agent being based on a serotonin 5-HT5A receptor regulating action.The inventors perfected the invention upon discovering that a tetrahydroisoquinoline derivative characterized by having a structure in which an acylguanidino group is bonded to an N atom of a tetrahydroisoquinoline ring, and a ring group is bonded to an unsaturated ring, has a powerful 5-HT5A receptor regulating action as well as an exceptional pharmacological action based thereon; and learning that the tetrahydroisoquinoline derivative is useful as an agent for preventing or treating dementia, schizophrenia, and other conditions.
US20080312277 Gpr41 and Modulators Thereof for the Treatment of Insulin-Related Disorders The present invention relates to a method for identifying a glycemic stabilizing compound by: a) contacting a candidate compound with GPR41, and b) determining whether GPR41 functionality is modulated, where a modulation in GPR41 functionality is indicative of the candidate compound being a glycemic stabilizing compound. In addition, the invention relates to a method for identifying a glycemic stabilizing compound, comprising: a) contacting a candidate compound with GPR41, and b) determining whether GPR41 functionality is increased, wherein an increase in GPR41 functionality is indicative of the candidate compound being a glycemic stabilizing compound. Further, the invention relates to a method for identifying a glycemic stabilizing compound, comprising: a) contacting a candidate compound with GPR41, and b) determining whether GPR41 functionality is decreased, wherein a decrease in GPR41 functionality is indicative of the candidate compound being a glycemic stabilizing compound.
CN102698272A Medicinal composition for preventing diabetes, and application thereof The invention relates to a medicinal composition for preventing diabetes. The medicinal composition comprises Alpha-glucosidase inhibitor and Semen Oroxyli (seed of Oroxylum Indicum (L.) Vent.) extract. The Semen Oroxyli extract is prepared by extracting Semen Oroxyli with aqueous solution of organic solvent, filtering, extracting, separating, and drying. The medicinal composition comprising Semen Oroxyli extract and Alpha-glucosidase inhibitor with dosage lower than normal dosage has good IGT (impaired glucose tolerance) improving effect manifested by rapidly and effectively lowering postprandial blood sugar and reducing blood plasma glucose toxicity; can better lower HbAlc (glycohaemoglobin) and TG (triglyceride) level; can reduce dosage of Alpha-glucosidase inhibitor, improve medicinaleffect, and effectively overcome the defects of existing diabetes preventive drugs in large side effects and weak intervention effect.
WO2014074997A1 Enzymes for inhibiting growth of biofilms and degrading same Enzymes for inhibiting growth of biofilms and degrading biofilms. The enzymes comprise glycosyl hydrolases capable of degrading biofilms. The enzymes are formulated in compositions with and without antimicrobial agents. The enzymes with and without the antimicrobial agents are delivered to biofilms to degrade the biofilms and treat infections of microorganisms associated with the biofilms, delivered to surfaces to inhibit growth of biofilms thereon, and administered to animals to inhibit growth of biofilms therein.
US20110105515 Targeting the oncoprotein nucleophosmin (+)-Avrainvillamide, a naturally occurring alkaloid with antiproliferative activity, is shown to bind to the oncoprotein nucleophosmin. Nucleophosmin is known to regulate the tumor suppressor protein p53 and is overexpressed in many different human tumors. The invention provides methods of modulating nucleophosmin and p53 using (+)-avrainvillamide and analogues thereof. These compounds may provide leads for the development of novel anti-cancer therapies that target nucleophosmin.
WO2006101454A1 Benzothiophene derivatives: preparation and pharmaceutical applications The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzothiophene containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).
US7807710 epothilone-like derivates used as anticarcinotgenic and antitumor agents The invention relates to the novel macrocycles of general formula (I) and to their use in the treatment of tumor diseases.
US20090022811 Mineralized guided bone regeneration membranes and methods of making the same The present invention provides a method for mineralizing commercially available guided bone regeneration membranes. The method comprises the steps of (a) providing a commercially available guided bone regeneration membrane, (b) applying a mineralizing solution, and (c) microwaving the membrane. The method may further comprise (d) rinsing the membrane in a solution such as distilled water and (e) drying the membrane. The mineralizing solution may be a solution capable of supplying or delivering a mineral such as calcium or zinc. The invention further provides guided bone regeneration membranes made by the methods described. The guided bone regeneration membrane comprises a mineral, such as, for instance calcium or zinc at a weight percent of at least 5%, at least 10%, at least 12%, at least 15%, at least 18%, at least 20% or at least 25% (weight percent) of the membrane. Further, the invention provides methods for enhancing bone regeneration and methods for inhibiting bacterial infection and inflammation.
CN102114019A Compound cefaclor preparation and preparation method The invention relates to a preparation of a medicine and a preparation method, in particular to a compound cefaclor preparation and a preparation method, and belongs to the technical field of pharmacy. The preparation is characterized by being prepared by adding a proper amount of pharmaceutical excipients into 25 to 35 weight parts of medicine, namely cefaclor and 0.5 to 1.5 weight parts of bromhexine hydrochloride, wherein the cefaclor is calculated based on anhydrous cefaclor, and the bromhexine hydrochloride is calculated based on bromhexine; and the excipients consist of a suspending agent, a flocculating agent, a flavoring agent and a flow aid. The invention provides a formula capable of improving the dissolubility and suspension stability of medicines and the mouthfeel of finished products, and a preparation technology.
WO2006054514A1 Preventive or therapeutic pharmaceutical composition for neuropathic pain A medicine useful for the prevention or treatment of neuropathic pain. There is provided a preventive or therapeutic pharmaceutical composition for neuropathic pain, comprising as an active ingredient a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative of the general formula (I) or a pharmacologically acceptable salt thereof. (I) In the formula, A is a lower alkylene; B is an amino, a di-lower-alkyl substituted amino, an alicyclic amino, etc.; n is an integer of 1 or 2; the carbon atom marked with * is a carbon atom of R-configuration or S-configuration, or a carbon atom having the same mixed therein; and the carbon atom marked with (S) is a carbon atom of S-configuration.
EP1863820A1 Thioamide-substituted tricyclic benzimidazoles useful for the treatment of gastrointestinal diseases The invention relates to cyclic benzimidazoles of formula (I), in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.
WO2007000779A3 Pharmaceutical sustained release compositions and processes thereof Pharmaceutical sustained release composition comprising at least one active agent(s), or its tautomeric forms, analogues, isomers, polymorphs, solvates, or salts thereof; preferably an antiviral active agent is provided. Also provided is a process of preparation of such composition and method of using them. The sustained release compositions of the present invention are able to deliver the active agent in a desired manner for an extended period of time.
WO2007135970A1 Heterocyclic type cinnamide derivative Disclosed is a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof. Also disclosed is a use of the compound or salt as a pharmaceutical product. (I) (In the formula, Ar1 represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like; Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group or the like; X1 represents -CR3=CR4- (wherein R3 and R4 respectively represent a C1-6 alkyl group or the like); and R1 and R2 respectively represent a C1-6 alkyl group or the like.)
WO2013150292A1 Composition for the treatment of inflammatory and immune disorders The invention relates to the treatment of an inflammatory or immune disorder with a pharmaceutical composition including methylsulphonylmethane, glucosamine and glycine or pharmaceutically acceptable salts or derivatives of these compounds.
US20080286382 Selenium, selenized yeast; gene expression inhibition The present invention relates to compositions comprising selenium (e.g., organic selenium (e.g., selenized yeast (e.g., SEL-PLEX))) and methods of using the same (e.g., as a therapeutic and/or prophylactic treatment). For example, the present invention provides compositions comprising selenium (e.g., organic selenium (e.g., selenized yeast (e.g., SEL-PLEX))) and methods of using the same for treating and/or preventing one or more conditions (e.g., problems) disorders, and/or diseases related to establishing and/or maintaining a pregnancy. Compositions and methods of the present invention find use in, among other things, research and clinical (e.g., preventative and therapeutic) applications.
CN101756998A Nasal pharmaceutical composition adopting cyclodextrin to include momestasone furoate The invention relates to a nasal pharmaceutical composition adopting cyclodextrin to include momestasone furoate. The nasal pharmaceutical composition comprises momestasone furoate and one or more pharmaceutically acceptable adjuvant materials, and is characterized in that the momestasone furoate as an active ingredient in the pharmaceutical composition is included by the cyclodextrin and/or a derivative thereof. The nasal pharmaceutical composition is used for treating allergic rhinitis of humans or mammals.
EP1339413B1 Compositions comprising complexes of phosphate derivatives of tocopherol There is provided a composition comprising the reaction product of: a) one or more phosphate derivatives of one more ore hydroxylated actives; and b) one ore more complexing agents selected from the group consisting of amphoteric surfactants, cationic surfactants, amino acids having nitrogen functional groups and proteins rich in these amino acids.
CN102247357A Application of uvarilactam and aristololactam BI in preparation of anticancer medicaments Relating to the technical fields of natural medicinal chemistry and medicines, the invention specifically relates to the application of two aistololactam compounds-uvarilactam and aristololactam BI in preparation of anticancer medicaments. Cytotoxic activity experiments by a MTT (methyl thazolyl tetrazolium) method conducted in the invention show that, uvarilactam and aristololactam BI present obvious inhibiting effects on human lung cancer cells and human intestine cancer cells, so that uvarilactam and aristololactam BI can be used for preparing anticancer medicaments, thus providing a new source for the seeking of anticancer medicaments.
EP1534847A1 Retroviral vector and stable packaging cell lines A retroviral vector comprising, and capable of expressing, a nucleotide of interest (NOI), wherein the NOI encodes a protein which is harmful to a cell.
CA2314942C Compositions and methods for increasing the concentration and/or motility of spermatozoa in humans A method is disclosed for treating idiopathic asthenozoospermia and improving sperm quality which comprises orally or parenterally administering to a subject in need thereof a combination preparation comprising either an admixture of or separately packaged L-carnitine and acetyl L-carnitine, or a pharmacologically acceptable salt thereof, in molar ratios ranging from about 4.0:1 to 1:1.5.
WO2012164473A1 3-spirocyclic piperidine derivatives as ghrelin receptor agonists The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
WO2011050481A1 New eremophilane sesquiterpene lactones from senecio jacobaea New eremophilane sesquiterpene lactones were isolated from the extract of the root of Senecio jacobaea having the general formula I. The structures were elucidated by spectroscopic methods including 2D NMR techniques. Methods of using the compounds as acetylcholinesterase inhibitors and neuroprotective compounds are also described
CN102596189A Use of guaifenesin for inhibiting mucin secretion A method of inhibiting mucus secretion in an individual that includes administering an effective amount of a composition which comprises guaifenesin.
US20090036521 Process for Production of Optically Active Amine Derivatives An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture.
US20060148844 Pharmaceutical composition for treatment of disease due to vascular constriction or vasodilation A therapeutic and/or preventing agent for a disease due to vascular constriction or vasodilation comprising a EDG-5 modulator. Since EDG-5 modulator specifically binds EDG-5 and shows antagonistic or agonistic action, EDG-5 antagonist is useful for treating and/or preventing for a disease due to vascular constriction, for example, cerebrovascular spasmodic disorder after subarachnoid hemorrhage or stroke, cardiovasucular spasmodic disorder, hypertension, renal disease, cardiac infarction, cardiac angina, arrhythmia, facilitation of the portal blood pressure involved in liver cirrhosis, varicosity involved in liver cirrhosis and the like, or EDG-5 agonist is useful for treating and/or preventing for a disease due to vasodilation of blood vessels, for example, chronic headache (such as migraine, tension-type headache, mixed-type headache thereof, or migrainous neuralgia), haemorrhoid, congestive disorder and the like.
CN103230381A Zolpidem tartrate time-selecting pulse sustained-release pellet and preparation method thereof The invention relates to the field of medical preparations, in particular to a zolpidem tartrate time-selecting pulse sustained-release pellet and a preparation method thereof. The pellet sequentially comprises a blank pill core, a medicine layer, a swelling layer and a time-lag layer from inside to outside, wherein the medicine layer comprises zolpidem tartrate, a surfactant and a binder. The swelling layer consists of two swelling materials. The time-lag layer is an ethyecellulose aqueous dispersion coating. Compared with the conventional technology, the preparation method has the advantages that stable 4 hours time lag and quicker pulse release of the pellet are provided, wherein the medicine release amount within one hour after lag-time is greater than 90%, so that the early awakening patient can be effectively prevented from waking up before dawn, and meanwhile, the residual effect in the next day can be avoided. The auxiliary material used in the preparation method of the pellet is easily available, and the production process is simple and easy to operate, so that the pellet is suitable for industrial production.
CA2145527C Tissue protective and regenerative compositions Methods are provided for preparing compositions suitable for protecting irritated or damaged skin from further oxidative and biochemical damage and thus permitting natural healing processes to progress, for accelerating the rate of healing of burns and surgical wounds, and for increasing the size of hair follicles and the rate of hair growth. The compositions generally comprise precipitates formed by the complexation of peptone digests of various proteins with copper(II) salts, indium(III) salts, tin(II) salts and tin(IV) salts.
WO2007090574A1 Protease inhibitor for wound treatment The present invention relates to protease inhibitors selected from the group of compounds which comprise iodine or iodophores for producing a composition for the treatment of chronic wounds.
US20120088742 Acetylsalicylic acid salts Novel betaine salts of acetylsalicylic acid, namely 4-trimethylammoniobutanoate acetylsalicylic acid addition salt (gamma-butyrobetaine acetylsalicylate), L-carnitine acetylsalicylic acid addition salt and 3-(trimethylammonioamino)propanoate (meldonium) acetylsalicylic acid addition salt. Use of meldonium acetylsalicylate as antiplatelet agent for treating various pathologies induced by platelet aggregation, anti-inflammatory and antihyperlipidemic agent.
US7176178 Protein H and its fragments/derivatives are capable of interacting with nucleophosmin/B23, actin, NPM/B23, protein SET or hnRNP A2/B1 A nuclear delivery construct comprises (i) protein H or a fragment or derivative thereof that is capable of being targeted to the nucleus of a eukaryotic cell; and associated therewith (ii) one or more other components whose targeting to the nucleus of the eukaryotic cell is desired.
WO2014036244A1 Methods of administering a 5,5-fused heteroarylene hepatitis c virus inhibitor for treating of preventing hepatitis c virus infection Provided herein are methods of administering a 5,5-fused heteroarylene hepatitis C virus inhibitor compound or an isotopic variant thereof, or a pharmaceutically acceptable salt or solvate thereof; for treating or preventing hepatitis C virus infection in a subject.
CN103751099A Bifonazole vaginal expansion suppository, as well as preparation method and detection method thereof The invention relates to a bifonazole vaginal expansion suppository, as well as a preparation method and a detection method thereof. The expansion suppository comprises a medicine-containing matrix formed by bifonazole and a matrix and an expansion carrier; polyethylene glycol 32 glycerol monolaurate, chitin, potassium sorbate, xylitan monostearate and monodecanoyl-glycerol are added into the medicine-containing matrix, and the prepared bifonazole vaginal expansion suppository has the beneficial effects of high stability, uniform dispersion of medicines, low irritation, high bioavailability, significant curative effect and the like; and furthermore, the provided bifonazole vaginal expansion suppository adopts six originally created leading technologies, and can prevent medicine liquid from flowing to the outside and prevent secondary infection.
CN102743408A Application of Cistanche deserticola polysaccharide in medicine preparation used for improving learning memory function The invention discloses an application of Cistanche deserticola polysaccharide in medicine preparation used for improving learning memory function, and is characterized in that a channel water labyrinth and a Morris labyrinth are used for respectively discussing the influences of the mouse learning memory acquired obstacle caused by Cistanche deserticola polysaccharide on the scopolamine hydrobromide, the mouse learning memory reproducibility obstacle caused by ethanol and the mouse learning memory consolidation obstacle, which show that the Cistanche deserticola polysaccharide has intelligence promotion effect, and the application provided by the invention makes a research for a effect mechanism that the Cistanche deserticola polysaccharide improves the learning memory function to reduce the mouse hippocampus and cerebral cortex AChE active content and increase the content of Ach in brain.
CN101129866A Method of preparing externally-painting medicine for treating zoster Disclosed is an externally-applied medicament for treating herpes zoster and its preparing process, wherein the medicament is prepared from the following raw materials (by weight portion): borneol 8-10g, alum 6-8g, and right amount of cold rice soup. The invention realizes easy material availability, simplified preparation, low cost, and quick effect.
CN1878768A Heteroaryl deravatives as PPAR activators This invention relates to compounds of formula (I), wherein one of R<6>, R<7> and R<8> is formula (II) and X, Y<1> to Y<4> , R<1> to R <14> and n are as defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPARdelta and/or PPARalpha agonists.
CN102727696A Ointment for treating burn and preparation method of ointment The invention discloses an ointment for treating burn and a preparation method of the ointment. The ointment is prepared by angelica sinensis, sinkiang arnebia root, radix sanguisorbae, rhizoma coptidis, rheum officinale, radix angelicae, sangusis draconis, beewax, calomel, borneol, catechu, colophony, castor seeds, olibanum and sesame oil; and the preparation method comprises the steps of weighing, crushing, dry-roasting and mixing and the like. The ointment has the advantages that the ointment is capable of relieving pain and healing the burn faster, and is safe without side and toxic effects and cheap in cost, thereby furthest releasing the physical or emotional pain for the patients suffered from the burn.
CN103463099A Application of Kadcoccitones A in preparing antibacterial medicines The invention relates to application of Kadcoccitones A in preparing antibacterial medicines. Kadcoccitones A has a strong effect in inhibiting escherichia coli, pseudomonas fluorescens, staphylococcus aureus, proteusbacillus vulgaris and cryptococcus neoformans, can be used as an antibacterial compound, is disclosed for the first time, has a strong activity for inhibiting bacteria, has a highlighted substantial characteristic, and is remarkably progressed when being used for preventing and treating bacterial infection.
WO2012051318A1 Sulphonamide compounds and methods of making and using same The invention provides sulphonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
CN1593416A Method for preserving and preparing hydroxycamptothecine ring closure injection Disclosed is a closed-loop method for conserving Hydroxy camptothecin which consists of, charging water into Hydroxy camptothecin, adjusting pH=9-12 by charging alkali, charging filler, stirring to dissolve, filtering with 0.22 mu microporous filtration film, charging acid or acidic amino acid solution to adjust pH=6.5-8, obtaining uniform emulsion, keeping the volume, split charging, and freeze-drying.
WO2012100734A1 Compounds useful as retinoid-related orphan receptor gamma modulators Disclosed are retinoid-related orphan receptor gamma (RORγ) modulators of Formula (I) and their use in the treatment of diseases mediated by RORγ, wherein the radicals have the meanings as defined in the invention.
US20060142249 Ophthalmic use The present invention relates to the use of a GABA-C-antagonist in the preparation of a medicament for the treatment of myopia.
CN101049307A Matrine eye drip liquid, and producing method An eyedrops of matrine for treating bacterial or viral keratitis and conjunctivitis, xerophthalmia, and eyeground arteriosclerosis is prepared through heating the water for injection, stirring while adding matrine and sodium chloride, regulating pH=6.5-7.5, stirring while sequentially adding ethyl p-hydroxybenzoate, sodium hyaluronate and the water for injection, boiling, aseptic filtering, cooling, and loading in containers.
WO2011113060A2 Antiviral compounds and methods of use thereof Inhibitors of retroviral propagation, methods of treatment and prevention of retroviral infections using the inhibitors, and pharmaceutical compositions including the inhibitors, are disclosed.
US7153865 N-type calcium channel antagonists for the treatment of pain Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R1, b, R3, d, R4, R5, R6 and R7 are any of a number of groups as defined in the specification, and pharmaceutical compositions and methods of treatment utilizing such compounds.
EP1904057B1 Hydroquinone ansamycins in the treatment of gastrointestinal stromal tumors The present invention provides methods for treating hyperproliferative disorders such as cancer by administering hydroquinone ansamycin compounds.
WO2007064619A1 Pyrimidine derivatives as hiv integrase inhibitors The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV. Formula (I)
WO2013163766A1 ANTIMICROBIAL COMPOSITIONS COMPRISING A HYALURONIC ACID BINDING PEPTIDE AND A β-LACTAM ANTIBIOTIC Compositions and methods for the treatment of antibiotic resiatant Staphylococcus aureus infections are provided comprising β-lactam antibiotics, as well as a hyaluronic acid binding peptide. The antibiotics include cephalosporins as well as the ηοη-β lactam antibiotic vancomycin. The methods provide administering the composition to the subject in an amount effective to reduce or eliminate the infection.
CN101203224B Use of pyrimidylaminobenzamides for the treatment of diseases that respond to modulation of Tie-2 kinase activity The present invention relates to the use of pyrimidylaminobenzamide compounds for the preparation of a drug for the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, especially for the curative and/or prophylactic treatment of leukemia, myelodysplastic syndromes or pulmonary hypertension, and to a method of treating diseases that respond to modulation of kinase activity, especially tie-2 kinase activity.
CN102206195A Crystalline quetiapine fumarate and pharmaceutical compositions thereof The invention relates to a method for producing crystalline quetiapine fumarate which is produced by using water as a solvent, heating, dissolving and cooling crystallization. The invention also discloses a preparation using crystalline quetiapine fumarate prepared by the method. A quetiapine fumarate tablet which is prepared by mixing the crystalline quetiapine fumarate with auxiliary materials, granulating the mixture, adding a lubricant into the granulated mixture and tabletting, has fast soluble speed, and is capable of effectively improving product bioavailability.
EP1328504B1 Aliphatic amino-substituted demethoxylated hypocrellins and their synthesis The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.
EP0748228B8 powder FOR THE PROVOCATION OF AIR PASSAGE NARROWING AND/OR THE INDUCTION OF SPUTUM A method as described for testing the susceptibility of a person to asthma. The person inhales an effective amount of sodium chloride, mannitol or another substance capable of altering the osmolarity of airway surface liquid in the subject. The substance is in the form of a dispersible dry powder containing an effective proportion of particles of a respirable size. The subject is then measured to detect airway narrowing which is indicative of a propensity for asthma. The same technique of dry powder inhalation can be used to test for the susceptibility of a person to rhinitus, to induce sputum and promote mucociliary clearance.
EP2019834A1 Ectonucleotidase inhibitors Present invention provides ectonucleotidase (ecto-nucleotide triphosphate diphosphohydrolase, NTPDase) inhibitors represented by the following formula, namely nucleotide mimetics as selective NTPDase inhibitors. It also provides methods for preparations of said compounds. Furthermore provided are pharmaceutical and diagnostic compositions comprising said compounds, and the use of said compounds in a medicament for treating diseases associated with ectonucleotidase activity and/or P2 receptors.
US20090203646 Use of sodium narcistatin for reducing internal adhesions and fibrosis The present invention concerns a method for reducing or preventing development of adhesions, fibrosis or scar tissue within serous body cavities by using sodium narcistatin.
CN103054824A Lurasidone hydrochloride orally-disintegrating tablet preparation and preparation method thereof The invention belongs to the technical field of medicine, and relates to a lurasidone hydrochloride orally-disintegrating tablet preparation and a preparation method thereof. The orally-disintegrating tablet comprises the following components in mass percent: 5-60 percent of lurasidone hydrochloride, 25-80 percent of filling material, 5-20 percent of disintegrating agent, 0.02-0.15 percent of wetting agent, 0.2-5 percent of flavoring agent and 0.5-2 percent of lubricating agent. The invention aims to provide a lurasidone hydrochloride orally-disintegrating tablet with simple preparation process, low cost, convenience in use and quick action to the indications; and compared with the conventional preparation for oral use, the lurasidone hydrochloride orally-disintegrating tablet preparation can reduce the difficulty in swallowing, improve the compliance, is suitable for special populations such as the elderly, children, patients with difficulty in swallowing and mental patients, can be fully disintegrated within 60 s, can be disintegrated into extremely fine powder, is higher in drug dissolution rate and quick in absorption, and can improve the bioavailability of insoluble drugs, for example, lurasidone hydrochloride.
US20100022478 Chiral compounds substituted with phosphonate acid ester functions or phosphonic acid functions The present invention relates to novel compounds that contain PNA units substituted with phosphonic acid ester functions or phosphonic acid functions, and have at least one chiral center. The compounds may be used for the treatment of viral diseases, such as AIDS.
US20090036496 Treatment of Stress Urinary Incontinence and Mixed Urinary Incontinence Use of a compound corresponding to formula (I): in which R represents hydrogen or a group chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene, cycloalkylidyne and —CONH2 groups, and —COR′ and —COOR′ groups, where R′ is chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene and cycloalkylidyne groups, it being possible for said groups R and/or R′ to be substituted and/or interrupted with —O—, —COO—, —OCO—, —NHCO— or —CONH— functions, or a pharmaceutically acceptable salt of said compound, for obtaining a medicinal product for use in the treatment of stress urinary incontinence and of mixed urinary incontinence.
US20100048594 Use of cytohesin inhibitors for chemically inducing longevity The invention relates to compounds selected from among the group comprising general formulas (1), (2), (3), and/or (4) and/or the enantiomers, diastereomers, and derivatives thereof, and the pharmaceutically acceptable salts thereof for producing a medicament used for therapeutically and/or preventively treating disease and pathological conditions linked to regulation of the insulin and/or insulin-like growth factor (IGF) signalling pathway and/or for chemically inducing longevity.
WO2007045009A1 Microbicidal dendrimer composition delivery system A microbicidal delivery system including: a microbicidal composition including a microbicidal compound including a dendrimer including one or more surface groups of formula (IV); a microbicidally active derivative thereof, or pharmaceutically acceptable salt or solvate thereof; and a carrier, excipient or diluent therefor; and a prophylactic device; the microbicidal composition being carried on a surface of the prophylactic device and being compatible therewith.
EP1429712B1 Method for treating bronchial constriction and bronchospasm The present invention is directed to a method for treating bronchial constriction in mammals. The method comprises contacting mammalian lung with a compound selected from the group consisting of pyruvate and pyruvate precursors. The compound is present in a therapeutically effective amount to produce bronchial dilation. The present invention is also directed to a method for treating airway disease in mammals. The method comprises contacting mammalian lung with a compound selected from the group consisting of pyruvate and pyruvate precursors. The compound is present in an amount from about 0.0001 millimoles to about 0.005 millimoles. The present invention is further directed to a method for treating airway disease in mammals. The method comprises contacting the mammalian lung with a compound selected from the group consisting of pyruvate and pyruvate precursors. The compound is present in a therapeutically effective amount to prevent bronchial spasm. The present invention is still further directed to a method for treating airway disease in mammals. The method comprises contacting the mammalian lung with a compound selected from the group consisting of pyruvate and pyruvate precursors. The compound is present in a therapeutically effective amount to prevent bronchial constriction.
CN102010432A Cefodizime sodium compound and novel method thereof The invention provides a cefodizime sodium compound and a novel method thereof. The purpose of refining purification is achieved by acid-base salifying reaction, activated carbon adsorption and chromatographic column adsorption separation purification, high-purity cefodizime sodium compound is finally obtained, the preparation product quality is improved, the toxic and side effects are reduced, and the safety in the preparation of broad spectrum antibacterial activity medicine usage is ensured; in addition, compared with the prior art, the method is simple, convenient and feasible in process, has low cost, high yield and high product purification, reduces toxic and side effects and is suitable for industrialized production.
CN102198136B Application of novel stable Ulifloxacin mesylate in preparing anti-infective medicament Because of poor solubility in water, Ulifloxacin has low bioavailability. The invention relates to a novel Ulifloxacin mesylate, a preparation thereof, a kit comprising the medical antibiotic preparation, and application of the novel Ulifloxacin mesylate in preparing an anti-infective medicament. The invention specifically relates to a novel medicinal preparation which is used for injection and remains stable in storage; the chemical name of the preparation is 6-fluorine-1-methyl-7-(1-piperazinyl)-4-oxo-4H-[1,3]thiadiazolebutane[3,2-a]quinoline-3-mesylate. In the invention, injection and administration are carried out directly in the form of Ulifloxacin mesylate, and therefore solubility and bioavailability of Ulifloxacin are enhanced, and treatment effects of the preparation are improvedsimultaneously.
CN103462982A Application of spirooliganones B in preparation of medicine inhibiting bacteria The invention discloses the application of spirooliganones B in preparation of the medicine inhibiting the bacteria. The spirooliganones B has good effect on inhibiting the escherichia coli, the pseudomonas fluorescens, the staphylococcus aureus, the proteusbacillus vulgaris and the cryptococcus neoformans, can be sued as an antibacterial compound and is disclosed for the first time. The spirooliganones B has the advantages of being high in inhibitory activity for the bacteria and prominent in substantive features, and makes remarkable progress in preventing infection of the bacteria.
CN101590065A Application of sibiricose A1, sibiricose A5 and tenuifoliside A in preparing tristimania treating products The invention discloses a new medicinal application of sibiricose A1, sibiricose A5 and tenuifoliside A, in particular to an application of sibiricose A1, sibiricose A5 and tenuifoliside A in preparing tristimania treating products. The sibiricosee A1, the sibiricose A5 and the tenuifoliside A have a better treatment function for tristimania caused by various reasons; the sibiricose A5 and the tenuifoliside A have a certain protecting function for PC 12 cells damaged by glutamic acid; and the sibiricosee A1, the sibiricose A5 and the tenuifoliside A all can shorten the tail-hanging resting time and the swim resting time of a mouse. Compared with a mould group, a dose group has marked difference in statistics and dose dependence and shows a better anti-depression effect.
CA2542835A1 Rna interference mediated inhibition of gene expression using short interfering nucleic acid (sina) This invention relates to compounds, compositions, and methods useful for modulating gene expression using short interfering nucleic acid (siNA) molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of genes, such as expressed pseudogenes associated with the maintenance or development of diseases, disorders, traits, and conditions in a subject or organism.
WO2013168803A1 Skin-improving agent A skin-improving agent which contains, as an active ingredient, an amino acid composition or the like, said amino acid composition containing 15-25% by weight of glycine or a salt thereof, 8-18% by weight of glutamic acid or a salt thereof, 5-15% by weight of proline or a salt thereof and 4-14% by weight of alanine or a salt thereof, respectively relative to the total amount of the amino acid composition. Another skin-improving agent, wherein the amino acid composition contains 50-100% by weight of glycine, glutamic acid, proline and alanine or salts of these amino acids in total relative to the total amount of the amino acid composition.
US20080255050 Administering 2-aminopurine or a pharmaceutically salt thereof; optionally also administering an additional hypolipidemic agent; 2-AP and nonphosphorylatable eIF-2 alpha mutant inhibit eIF-2 alpha phosphorylation, inhibit foam cell formation and atherosclerosis development A method of treating atherosclerosis in a subject is carried out by administering the subject 2-aminopurine or a pharmaceutically salt thereof in a treatment effective amount. Optionally, the subject may also be administered an additional hypolipidemic agent. Compositions useful for carrying out the present invention are also described.
EP1544281A1 Fat composition The present invention relates to an oil or fat composition containing the following components (A) and (B): (A) from 80 to 99.9 wt.% of a monoglyceride comprising 20 to 75 wt.% of docosahexaenoic acid (DHA) and 0.1 to 25 wt.% of icosapentaenoic acid (IPA), as the constituent fatty acids thereof, wherein the weight ratio of DHA/IPA being 2 or more; and (B) from 0.1 to 20 wt.% of a diglyceride. The oil or fat compositions according to the present invention are excellent in processability, have a good flavor, and are excellent in PPAR activating effects and β oxidation activating effects so that they are beneficial as foods and animal feeds as well as pharmaceuticals for diabetes, hyperlipidemia and obesity.
US20050171026 Inhibiting SF2/ASF-dependent splicing of beta-globin pre-mRNA in vitro by suppression of Clk-mediated phosphorylation of SR proteins (serine/arginine-rich); a benzothiazole, TG003, is inhibitor of Clk/Sty(CDC2-like kinases); anticancer, antitumor; neurodegenerative diseases The present invention provides a composition of treating, preventing abnormal splicing caused by the excessive kinase induction, which comprises TG003 and a method using the same of treating, preventing abnormal splicing caused by the excessive kinase induction.
WO2009080025A1 Compressed chewing gum comprising metformin The present invention relates to compressed medicament-containing chewing gum compositions. In particular, the present invention is directed to compressed chewing gum compositions comprising metformin. Such compositions are useful in the treatment of diabetes or ameliorating the symptoms of diabetes, in particular diabetes type II.
US7351531 Molecules capable of binding to telomere and the like and method with the use of the same A method of forming a self-connective structure (a hairpin structure, a four-stranded structure, etc.) of a single-stranded oligonucleotide chain by forming a mimetic base pair of a mismatch base pair failing to form any normal base pair among base pairs of the single-stranded oligonucleotide chain with the use of a compounds represented by the following general formula (I): A-L-B (I) wherein A represents a chemical structural moiety capable of forming a pair with one base of a base pair failing to form any normal base pair; B represents a chemical structural moiety capable of forming a pair with the other base of the base pair failing to form any normal base pair; and L represents a linker structure by which the chemical structures A and B are linked to each other; and a method of inhibiting the activity of enzyme according to the previous method.
US20050020637 Using reverse proton pump inhibitor The invention relates to the use of reversible proton pump inhibitors in the treatment of airway disorders.
US7435729 using estrogen antagonist ; anticancer agents Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-β over ER-α. Methods are disclosed for modulating ER-β in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-β. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
CN101125131A Method for preparing flupentixol and melitracen capsule The present invention relates to a preparation method of flupentixol - melitracen capsules, which is characterized in that the present invention adopts a ball milling machine to mix and grind the prescription dose of flupentixol dihydrochloride and the diluents to the powder, the preparation technique does not use the ethanol or solvent media, which can not only introduce no other organic impurities, but can also improve the bioavailability of the drug, so the present invention is more safe and effective for the human body.
US20080267969 Treatment of Pulmonary Hypertension Using an Agent That Inhibits a Tissue Factor Pathway An improved non-human animal model of severe pulmonary arterial hypertension (PAH) and its use for testing of therapeutic agents that can treat symptoms of PAH are disclosed. In addition, the present application relates to the identification of several classes of therapeutic agents that, alone or in combination, can be used to treat or prevent PAH or at least reduce the severity of symptoms associated therewith. Both gene therapy and non-gene therapy approaches are described.
US20080214639 Leuprolide acetate and acetylcholinesterase inhibitors/NMDA receptor antagonists for the treatment of alzheimer's disease Methods of treating, mitigating, slowing the progression of, or preventing Alzheimer's Disease include administration of gonadotropin-releasing hormone analogues in combination with acetylcholinesterase inhibitors and/or N-methyl-D-aspartate receptor antagonists.
US20120142675 Methods for Treating Diseases of the Retina Disclosed herein is a method of treating disorders of the retina comprising administering to a patient in need of such treatment a compound selected from the group consisting of olanzapine, certain of its metabolites, clozapine, and n-desmethyl clozapine.
CN101385705A Preparation method of aqueouse solution agent of minoplatin and other platinum complexes A method for preparing aqueous solution dosage forms of minoplatin and other platinum complexes belongs to the field of platinum complexes. The minoplatin can not be stable in aqueous solution for a long time, thus the minoplatin directly used for injection or transfusion cannot be prepared. In the present invention, the minoplatin is dissolved in a ligand thereof, namely cyclopentane-dicarboxylic acid at the mass ratio of 12:1-1:1, and added with sodium hydroxide to regulate pH to 5.5-7.0 to make the aqueous solution dosage form of the minoplatin. Likewise, carboplatin is dissolved in a ligand thereof, namely cyclobutane-dicarboxylic acid solution, and added with the sodium hydroxide to regulate the pH to 5.5-7.0 to make the aqueous solution dosage form of the carboplatin; or oxaliplatin is dissolved in oxalate solution, and added with the sodium hydroxide to regulate the pH to 5.5-7.0 to make the aqueous solution dosage form of the oxaliplatin. The aqueous solution dosage forms are stored in a closed container which can prevent ultraviolet radiation. Stability dynamics tests prove that more than six years is needed to decompose 1% of the aqueous solution dosage forms, thus any decomposition does not actually occur in the aqueous solution dosage forms of the minoplatin complex and other platinum complexes in the shelf life of two years.
US20070185128 Compounds and compositions for treating obesity Described herein are novel and useful compounds of the general formula Compounds of this invention can advantageously exhibit melanocortin receptor agonist activity. New and useful compounds comprising such a chemical structure and methods of modulating melanocortin receptor activity in a subject (and promoting, inducing, and/or enhancing the treatment or prevention of related diseases) by administering such a compound or composition also are described.
CN103330701A Applications of alkylaryl ketone The invention relates to applications of an alkylaryl ketone, and specifically relates to applications of a compound represented by formula I or pharmaceutically acceptable salts of the compound in preparing a medicament used for prevention or/and treatment of obesity. It is shown in formula I that: R1 to R5 are one respectively and independently selected from hydrogen, hydroxyl or C1-C3 alkyloxy; A is bivalent C4-C5 straight chain or branched-chain hydrocarbons; R6 is phenyl, substituted phenyl, 5-membered to 6-membered nitrogen containing heteroaryl or substituted 5-membered to 6-membered nitrogen containing heteroaryl; wherein the substituent of the substituted phenyl or the substituted 5-membered to 6-membered nitrogen containing heteroaryl is one or more than two selected from carboxyl, amido, sulfonic acid group, C1-C3 alkyl, C1-C3 alkyloxy or hydroxyl.
CA2753604A1 Drug combinations containing pde4-inhibitors and nsaids The present invention relates to new drug combinations which contain in addition to one or more PDE4-inhibitors at least one NSAID (= non-steroidal anti-inflammatory drug)(2), processes for preparing them and their use in treating in particular respiratory complaints such as for example COPD, chronic sinusitis and asthma. The invention particularly relates to those drug combinations which contain, in addition to one or more, preferably one PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 have the meanings given in claim 1, at least one NSAID (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.
US20090010894 Methods and systems for identifying compounds that modulate alpha-synuclein aggregation This invention relates to the field of determining the ability of agents to interfere with, reverse, or prevent α-synuclein aggregation and α-synuclein-related pathology and behavior. This invention also relates to methods for screening candidate agents for their potential as human medicaments.
US20110044971 Method and composition for treating a seratonin receptor-mediated condition A method and composition for treating serotonin receptor-mediated conditions.
WO2007071444A3 Esomeprazole arginine The esomeprazole arginine as well as processes for its preparation and pharmaceutical compositions containing it are described.
US20080247987 devices, and methods for the production, use and administration of the composition having a non-thermoreversible block copolymer composition. The present invention describes compositions, devices, and methods for the production, use and administration of the composition having a non-thermoreversible block copolymer composition.
EP2563367A1 Methods of treating retroviral infections and related dosage regimes The present invention relates to compounds and methods for treating retroviral infections and/or Hepatitis B viral infections. Some compounds of the invention are described by Formula (I) or a stereoisomer, a diastereomer, an enantiomer or racemate thereof.
WO2010141273A1 DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
CN102627669A Phosphate ester-containing piperazine derivative and preparation method as well as application thereof The invention relates to a phosphate ester-containing piperazine derivative and a preparation method as well as application thereof, in particular to one type of phosphate ester-containing piperazine derivatives with a structure shown by a formula I and a preparation method thereof, a medicinal composition with the phosphate ester-containing piperazine derivative with the structure shown by the formula I as an active ingredient and application thereof to preventing or treating diseases related to arginine vasopressin V1a receptors, arginine vasopressin V1b receptors, arginine vasopressin V2 receptors, a sympathetic nervous system or a renin-angiotensin-aldosterone system.
CN102850424A 3-Hydroxyprogesterone-21-(2',5'-dimethoxy)benzylidene-5-ene-20-one and preparation method and application thereof The present invention relates to a steroidal compound of 3-hydroxyprogesterone-21-(2',5'-dimethoxy)benzylidene-5-ene-20-one shown in structural formula I and preparation method thereof, a medicinal composition containing the compound, and the application of the compound in preparation of medicines for prevention and/or treatment of neurodegenerative diseases.
WO2013126797A1 Cholecystokinin b receptor targeting for imaging and therapy Conjugates are described herein where CCK2R targeting ligands are attached to an active moiety, such as therapeutic agent or an imaging agent, through a linker. The conjugates can be used in the detection, diagnosis, imaging and treatment of cancer.
US20100172952 Electrospun Scaffolds And Methods Of Generating And Using Same A porous scaffold is disclosed, the porous scaffold comprising electrospun polymeric nanofibers, wherein an average diameter of a pore of the porous scaffold is about 300 μm is disclosed. An average diameter of the polymeric nanofibers ranges from about 100 to 400 nm. The scaffold may comprise a plurality of particles, the particles being greater than about 1 μm in diameter. Methods of fabricating scaffolds, methods for generating tissue and methods of using scaffolds for tissue reconstruction are also disclosed.
EP2688871A1 Prodrugs of lxr modulating imidazole derivatives Imidazole prodrugs, pharmaceutically acceptable salts, or isomers thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
WO2009150381A3 Azacarboline derivatives, preparation thereof, and therapeutic use thereof as kinase inhibitors The invention relates to novel azacarbolines having formula (I), wherein R3, R4 independently represent H, hal, CF3, substituted oxy, optionally substituted alkoxy, optionally substituted amino, substituted carbonyl, optionally substituted carboxyl, optionally substituted amide, sulphur, such as optionally substituted sulphides, sulphoxides or sulphones, linear, branched or cyclic C1-C10 alkyl optionally comprising an optionally substituted heteroatom, optionally substituted linear, branched or cyclic C2-C7 alkenyl, optionally substituted linear or branched C2-C6 alkynyl, optionally substituted aryl or heteroaryl, optionally substituted heterocycloalkyl, R6 represents heteroaryl, C(O)NR1aR1b, heterocycloalkyl or -C(O)heterocycloalkyl, all of which may be optionally substituted; in the form of a base or an acid addition salt. The invention also relates to the therapeutic use of said azacarbolines for the treatment of cancer and to synthesis methods.
EP2366397A1 Intravascular indwelling catheter lock solution containing acetic acid and container containing the same A catheter lock solution which is a catheter lock preparation having a bacteriostatic property at physiological osmotic pressure without practically containing a bacteriostatic component such as a preservative, an antimicrobial agent, or an antibiotic and having high safety, characterized in that the preparation contains a weak acid having an acid dissociation constant (pKa) of 3.0 to 6.5 as a buffer, a pH of the solution is less than 6.0, preferably from 3.0 to about 5.5, an osmotic pressure ratio is from 0.5 to 3.0, and a pH change (variation) can be suppressed to less than the 6.0 with the weak acid, and a container containing the catheter lock solution.
CN101229309A Medicine for increasing sow fertility rate and preparing method thereof The invention relates to a medicine for improving farrowing rate and a production method thereof. The medicine is characterized in that the weight parts of the raw materials are: radix codonopsitis of 1 to 3, milk veteh of 1 to 3, atractylodes macrocephaia of 1 to 3, angelica of 2 to 4, yam of 1 to 3, green chiretta of 0.5 to 2, plaster of 0.5 to 2, balloonflower of 1 to 4, coptis root fried with wine of 0.5 to 2, baical skullcap root fried with wine of 1 to 3, houttuynia of 0.5 to 2, forsythia of 0.5 to 2, liquorice of 1 to 4, southernwood of 1 to 3, woad root of dyer of 0.5 to 2, magnolia officinalis of 0.5 to 2 and herba oldenlandiae of 0.5 to 2. The medicine has the advantages of an exclusive prescription, scientific and sophisticated materials, and simple and practical production method. The medicine produced can improve farrowing rate and by practical application, the average number of pigs per birth is above 11 to 12 pigs after sows take the medicine.
WO2014142507A1 Composition for preventing or treating colon cancer, containing 3,6-anhydro-l-galactose The present invention relates to a composition for preventing or treating colon cancer, containing 3,6-anhydro-L-galactose, and more specifically, provides excellent anti-cancer effects by inducing apoptosis of colon cancer cells and inhibiting the growth of colon cancer cells by using 3,6-anhydro-L-galactose separated from red algae-derived agar and purified.
EP1676575A2 Mucin production inhibitor To provide a drug useful for prevention or treatment of respiratory diseases accompanying hyper-secretion of mucus, the drug normalizing physiological functions of the respiratory tract by preventing over-production of mucin from the respiratory tract epithelium. A mucin production inhibitor comprising, as an active ingredient, a benzimidazole derivative represented by formula (1) : (wherein A represents a triazole group; R1 and R2 may be identical to or different from each other, and each represents an aliphatic hydrocarbon group which may have an alicyclic hydrocarbon group, or an alicyclic hydrocarbon group; R3 represents a hydrogen atom or a substituent; and R4 represents a hydrogen atom or a protective group for the nitrogen atom) or a pharmacologically acceptable salt thereof.
CN1966001A Medicament for treating inflammation and preparation method thereof The invention relates to a pharmaceutical composition for treating inflammation and process for preparation, wherein the process consists of steps of obtaining main constituents of the medicament through diacolation extracting, charging pharmaceutically acceptable auxiliary materials, making medicinal preparation through the conventional process. The obtained medicament can be used for treating inflammation caused by bacillus pyocyaneus infection, burns and scalds.
CN1569196A Rhodiola sacra injection and its preparation The invention provides a Rhodiola sacra active ingredient extract and its preparation, wherein the active ingredient extract mainly comprises Salidroside, flavones and polysaccharides, The invention provides injection preparation by using Rhodiola sacra effective position extract as the main raw materials and its preparation.
CN103601698A Benzothiazole compounds and application thereof The invention belongs to the technical field of medicine and relates to novel benzothiazole compounds capable of inhibiting gastric acid secretion and resisting Helicobacter pylori. The compounds effectively bind with the H+K+-ATP enzyme in vivo so as to eventually inhibit gastric acid secretion, and the compounds have good gastric acid inhibiting and anti-gastric ulcer activity. The structural formula (I) of the compounds is described in the specification, and R, m and n in the formula (I) are defined in claim 1.
CN101461944B Magnetic polyacrylic acid modified carbon nano-tube medicament carrier The invention belongs to the field of molecule biological medicine, and relates to a magnetic polyacrylic acid-modified nanometer pipe and a method for preparing the same. A multi-wall carbon nanometer pipe is modified by polyacrylonitrile and hydrolyzed under acid condition to obtain a polyacrylic acid-modified water-soluble nanometer pipe containing large quantity of carboxyl groups; by the water-phase chemical co-precipitation method, a magnetic ferroferric oxide-polyacrylic acid-modified multi-wall carbon nanometer pipe composite with the diameter of between 10 and 80nm is prepared, and the composite has good lymphotaxis and strong magnetic response; tests show that a medicine carrier can effectively adsorb chemical treatment medicines to a lymphatic system, slowly release the chemical treatment medicines in a metastasis lymph node of a malignant tumor, has good magnetic field positioning effect and obviously inhibits the proliferation and metastasis of the tumor cell of the lymphnode. The invention provides a novel intervention means for lymphatic metastasis of the malignant tumor.
CN103720674A Famotidine floating-adhesive micro-tablet capsule and preparation method thereof The invention discloses a famotidine floating-adhesive micro-tablet capsule and a preparation method thereof, belonging to the technical field of medicine. The preparation comprises famotidine, hydroxypropyl methylcellulose K4M, carbomer 971P, sodium bicarbonate, microcrystalline cellulose and magnesium stearate. A prepared famotidine floating-adhesive micro-tablet projects towards an outer circle, is 3 millimeters in diameter, and can be filled into a hollow hard capsule. The famotidine floating-adhesive micro-tablet can float in artificial gastric juice within 1 minute, floats continuously up to over 8 hours, and has certain adhesion. The release amount of the prepared famotidine floating-adhesive micro-tablet in 0.1M HCl solution within 1 hour is 50 percent less than a labelled amount. The preparation prolongs the retention time of famotidine in the stomach, so that the aims of reducing the administration times and enhancing the curative effect are fulfilled, and a novel selectable dosage form is provided for the development of a famotidine sustained-release preparation.
US7208283 Contacting with Ewing sarcoma protein and nuclear receptor; determining binding and changes in ligand-induced activity; use in diagnosis and treatment In the method of determining hormonal effects of substances, a test substance is contacted with Ewing sarcoma protein (EWS) or a derivative of it and with an androgen receptor (NR) or a derivative of it; and the effect of the test substance on binding of EWS with the androgen receptor or its derivative or on ligand-induced activity of the androgen receptor is determined, preferably in a cellular system. A method for determining interference in the co-modulator mechanism between androgen receptor and EWS, which includes measurement of androgen receptor and EWS concentrations, is described. A method for identification and characterization of substances that influence the activity of a nuclear receptor, especially androgen receptor, using EWS or a derivative of it is disclosed.
WO2010033043A8 Dendrimeric compounds comprising amino acids, hyperbranched core compound, process for preparation of dendrimeric compounds comprising amino acids and hyperbranched core compound, and use thereof The invention provides dendrimeric compounds of the formula 1 comprising amino acids, wherein n is an integer of 1-4, T is an alkylidene -(CH2)2CONH(CH2)2- group, R2 is an -NH2 group or a moiety of a primary organic amine, and P is an amino acid and/or peptide moiety, wherein at least one hydrogen atom of at least one amino group is optionally replaced by a protective group, and a hyperbranched core compound of the formula 3, wherein T and R2 are as defined above. The invention provides also a process for the preparation of a dendrimeric compound and a hyperbranched core, wherein the process employs addition reactions of alkyl acrylate and a basic amino acid, and use of a hyperbranched core for the preparation of a dendrimeric compound comprising amino acids. The invention provides also use of dendrimeric compounds for the preparation of the medicament for inhibiting growth of bacterial cells, fungi and tumor cells.
US20120245168 Composition, Synthesis, and Use of New Substituted Pyran and Pterin Compounds The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency.
CN101284100A Chinese caterpillar fungus compound capsules for prolonging and keeping the youth The invention belongs to the technology field of Tibetan medical health food, particularly a soft capsule prepared from Tibetan worm grass extract, Tibetan lamb placenta tissue hydrolysate, Tibetan saffron extract, Tibetan medlar extract, Tibetan royal jelly extract, Tibetan solomonseal extract, Tibetan milk vetch extract, Tibetan sea buckthorn extract, seaweed extract, coix seed extract, lycopene, etc. The preparation process for the soft capsule includes mixing the materials, stirring; filling into capsules, sealing; checking; and packaging to obtain finished product. The capsule is effective in improving immunity, caring skin, postponing aging, etc.
CN1813690A Asarone injection emulsion and its preparing method The present invention relates to an asarone injection emulsion and its preparation method. Its composition includes active component asarone and medicinal auxiliary material which can be selected from injection vegetable oil, emulsifying agent and isoosmotic regulating agent. Said asarone injection emulsion can be used for resisting bacteria, relieving inflammation, stopping cough, expelling phlegm, relieving asthma, relieving convulsion and resisting epilepsy, etc.
CN101302171A Production process of pure amino acid chelate and use thereof The invention provides a method for producing pure amino acid chelate and use thereof. The method is as followings: the first step is to reacting oxide or metal hydroxide and the amino acid to generate hydroxyl amino acetate; the second step is to conduct a combination reaction of the hydroxyl amino acetate which is generated in the first step and at least an amino-containing compound, and the compound with abundant amino is reacted with a metal ion, thus, the generated amino acid chelate structure is formed by combining one metal ion and a plurality of ligands of the amino acid, but the number of the ligands of the amino acid is equal to the number of the ligands of the metal ion, and the pure amino acid chelate is separated from reaction generation liquid. The second step also comprises several continuous sub-steps for reaction with a plurality of amino-containing compounds. The generated pure amino acid chelate can be applied to beverage, food, health products and medicine, in particular a zinc amino acid chelate that can obviously and effectively increase a white mouse immune function with lower immunity.
WO2014047323A1 Methods for treating post-traumatic stress disorder Embodiments of the invention generally relate to methods and supplements for treating post-traumatic stress disorder in human beings. Other embodiments of the invention generally relate to methods and supplements for improving sleep efficiency in human beings.
CA2133337C Compounds useful for treating allergic or inflammatory diseases Novel cyclohexanes of formulas (I) and (II) are described herein. They inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; these compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV.
US20110165218 Therapeutic Bone Growth and Regeneration The use of Herapan Sulphate 2 (HS-2) in therapeutic bone growth and regeneration is described. Herapan Sulphate 2 was identified as a variant of Heparan Sulphate purified from embryonic day (E10) of murine neuroepithelia.
CN1762385A Eye gel or in-situ gel and preparation method thereof The invention relates to an eye gel or in-situ gel and preparation method, comprising base compositions and auxiliary materials, wherein the base compositions include pearl powder extract, borneo camphor, tinkalite, boric acid, ethanol, gel base and glycerine, the auxiliary materials include osmoregulation agent and bacteriostatic agent.
CN103083358A Vitamin D-containing calcium preparation and preparation method thereof The invention discloses a vitamin D-containing calcium preparation and a preparation method thereof. The method comprises the following steps: (1) pre-mixing vitamin D particles with an average particle size of 150-300 mum and microcrystalline cellulose to obtain a premix; (2) mixing microcrystalline cellulose, a calcium salt and the premix to obtain a sub-premix; and (3) forming the vitamin D-containing calcium preparation from the sub-premix.
WO2011148962A1 Novel heterocyclic compound or salt thereof Disclosed is a medicament having a strong antibacterial activity against Gram-positive bacteria, Gram-negative bacteria, and resistant bacteria. A compound represented by formula [I] or a salt thereof is useful as an antibacterial agent. In formula [I], a bond containing a dotted line and connecting X2 to Y1 represents a single bond or a double bond; Z1, Z2, Z3, Z4, Z5, and Z6 each represent a nitrogen atom, formula: CH, or the like; X1 represents a C1-4 alkylene group which may be substituted by an oxo group; X2 represents a bonding hand or formula: CH; Y1 represents a spirocyclic group selected from a group of formulae (II); X3 represents a C1-4 alkylene group, formula: NR10(CH2)m, formula: SOn, or a bonding hand; and R7 represents a C3-6 cycloalkyl group, a C3-6 cycloalkenyl group, an aryl group, a monocyclic heterocyclic group, a bicyclic heterocyclic group, or the like.
WO2009085988A1 Salts of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7- dihydro-5h-pyrrolo[3,4-b]pyrazine Novel mesylate, (R)-mandelate, succinate, citrate, fumarate, D-malate, D-tartrate, sulfate and L-tartrate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
US20130028955 Sustained release oral matrix and methods of making thereof A solid dosage form suitable for forming a tablet for the containment and delivery of medicament is provided wherein the matrix forming material is a pressure sensitive adhesive, present in the amount from about 0.1 to about 40 weight %, based on the total weight of the composition. The dosage form is comprised of the medicament and a water-insoluble polymer silicone pressure sensitive adhesive and allows release of the medicament in a controlled fashion depending on simple parameters such as weight percent of the polymer silicone adhesive. A sustained release dosage form is provided for delivery of medicament wherein the release rate of medicament does not depend on the dissolution medium of the pH. Another aspect of invention is formation of solid tablets of poorly compressible material and the method for making the solid composition. The dosage form for this invention s particularly suitable for oral dosage forms.
CN103006911A Drug capsule for clearing away heat and loosing bowels and dispelling wind and relieving pain The invention discloses a drug capsule for clearing away heat and loosing bowels and dispelling wind and relieving pain. The drug capsule is prepared from coptis root, weeping forsythia capsule, peppermint, inula flower, baical skullcap root, fineleaf schizonepeta herb, cape jasmine fruit, divaricate saposhnikovia root, amur corktree bark, chrysanthemum, fried shrub chastetree fruit, liquorice root, Sichuan lovage rhizome, rhubarb root and rhizome, gypsum, platycodon root, dahurian angelica root, fineleat schizonepeta oil, peppermint oil, forsythia suspansa oil, crude drug fine powder, dextrin and magnesium stearate, and is characterized in that when net drugs are extracted, the weight ratio of coptis root to weeping forsythia capsule to peppermint to inula flower to baical skullcap root to fineleaf schizonepeta herb to cape jasmine fruit to divaricate saposhnikovia root to amur corktree bark to chrysanthemum to fried shrub chastetree fruit to liquorice root to Sichuan lovage rhizome to rhubarb root and rhizome to gypsum to platycodon root to dahurian angelica root to dextrin to magnesium stearate is 5:40:20:10:40:40:40:20:20:80:40:20:20:160:20:40:40:30:2.8. The drug capsule has the advantage that a better medical treatment effect is achieved.
US20120121533 Nucleic acid ligands to ll37 The present invention is directed to nucleic acid ligands to LL37, methods for producing said nucleic acid ligands, and methods for utilizing said nucleic acid ligands. In one exemplary embodiment, for example, this invention relates to nucleic acid ligands exhibiting high specific binding affinity to LL37 peptides, precursors and/or portions thereof. Further, the nucleic acid ligands may bind competitively with native ligands of LL37 and may also inhibit and/or interfere with LL37 function, such as by binding to LL37.
CA2290421C Multicyclic erythromycin derivatives Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having formulae (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), or (XI), pharmaceutical compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of formula (I).
US7045626 Quinoline derivatives, process for preparing them and use for the treatment of diseases mediated by s-CD23 A compound of formula (I): useful in the treatment and prophylaxis of conditions mediated by s-CD23
WO2005026171A1 Substance which exhibits antiviral and antibacterial activity and is based on derivatives of 2,8-dithioxo-1h-pyrano[2,3d¸6,5-d']dipyrimidyne and 10-aza-analogue thereof The invention relates to organic chemistry and medicine, more specifically to synthetic pyrimidine derivatives, i.e. 2,8-dithioxo-1H-pyrano[2,3d¸6,5-d']dipyrimidyne and 10-aza-analogue thereof and to the complexes and salts thereof which exhibit antiviral and antimicrobial activity. Said invention can be used for medicine and veterinary science for treating viral diseases, bacteria-induced diseases and for cosmetology in the form of an additive for preventing and treating infections. The aim of said invention is to develop a novel more efficient substance exhibiting antiviral and antimicrobial activity. The inventive substance which exhibits antiviral and antimicrobial activity is based on derivatives of 2,8-dithioxo-1H-pyrano[2,3d¸6,5-d']dipyrimidyne and 10-aza-analogue thereof and characterised in that it comprises the derivative of said group of general formula A1 ∗ M: wherein X is selected from a group O, NH, N-Alkyl; R1 is selected from a group H, Oh, Cl, O-Alkyl, NH2, NH-Alkyl; NH-Ar, N(Alkyl)2, SH, S-Alkyl, S-Ar, S-Hetaryl; R2 is selected from a group C6H5, Aryl; R3 is selected from a group H, Cl, O-Alkyl; NH2, NH-Alkyl, NH-Ar, S-Heratyl; M is absent or selected from a group of Na, K, Li, ammonium cation or another pharmacologically acceptable cation; or said complex of pharmacologically acceptable cation with the anion of one of derivatives A1 (above-mentioned variants R1-R3).
WO2013059232A1 Methods and compositions for the management of cancer using 2-dg and an igf-ir inhibitor The disclosure relates to methods and compositions for the management of cancer. In certain embodiments, the disclosure relates to methods of treating or preventing cancer by administering an IGF-IR inhibitor and 2-deoxyglucose to a subject in need thereof.
CA2221495C Methods and uses for apoptin This invention describes that apoptin fails to induce apoptosis in human normal cells. Besides, the invention describes that when normal cells are transformed, they become susceptible to the apoptin-induced apoptosis. The invention describes that apoptin induces in various human tumor cells a p53-distinct type of apoptosis, and cannot be blocked by a variety of apoptosis-inhibiting agents. The invention comprises an anti-tumor agent, which specifically kill tumor and not normal cells. It further provides the induction of cell death by means of gene therapy. Apoptin can induce apoptosis in non-human animal tumor cells. The invention also provides that in normal cells apoptin was found predominantly in the cytoplasm, while in tumor cells it was located in the nucleus. Besides, the invention comprises a diagnostic test for the determination of cell-transforming activity.
WO2007095618A3 Benzo-fused heterocycle sulfamide derivatives for the treatment of migraine The present invention is a method for the treatment or prevention of migraine comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined. The present invention is directed to a method for the treatment and / or prevention of migraine, which includes mono-therapy and alternatively, co-therapy with at least anti-migraine agent.
WO2012061415A1 Oxypyrimidines as syk modulators The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
CN102807558A Fluorine-containing dihydroindene amide compound used as protein kinase inhibitor The invention discloses compounds used for curing or preventing diseases related to protein kinase shown in the formula (I), medicinal salt thereof or a configurational isomer thereof, wherein a linking group L1, loops A, B and C and substituents R1, R2, R3, R4 and R5 are as defined in the specification. The invention also discloses a preparation method of the compounds shown in the formula (I), a medicine composition and applications of medicine prepared by the compounds for curing or preventing the diseases related to the protein kinase.
EP1703919A1 Vaginal compositions for treating infections This invention relates to methods, compositions and treatment regimens for applying cooling active ingredients to the perineum of a woman to treat the symptoms of a vaginal or vulvar infection or vulvar pain in order to speed the woman’s relief from pain and/or itch.
EP1773344A1 Cyclic progestin regimens and kits A method of contraception is provided which involves delivery of 21 to 27 consecutive days of a progestin in the absence of an estrogen or other steroidal compound, followed by 1 to 7 days without an effective amount of an active agent. Also described is a pharmaceutically useful kit to facilitate delivery of this regimen.
CN103415291A Methods of converting a patient's treatment regimen from intravenous administration of an opioid to oral co-administration of morphine and oxycodone by using a dosing algorithm to provide analgesia A method of converting a treatment for pain comprising intravenous administration of opioids, to a treatment for pain comprising oral administration of a first dose of an immediate release mgrphine-oxycodone combination in patients in need of analgesia, is disclosed. The method may comprise (1) determining a four-hour average oral morphine equivalents, a one-hour average oral morphine equivalents, or determining a net average hourly inlravenous dose, and (2) orally administering to the patient a first dose of a morphine-oxycodone combination in a 3:2 ratio by weight every four to six hours. Also, a method of treating pain in patients who had been administered opioids intravenously, comprises using a dosing algorithm to determine the first dose of the immediate release morphine-oxycodone combination.
US20100172950 Pharmaceutical compositions comprising dextran with a molecular weight of 1.0-100 kda and processes for their preparation A solid or semisolid implant obtainable by providing a liquid composition comprising an aqueous solution of dextran with molecular weight of 1.0-100 kDa and introducing the liquid composition into the body of a mammal, whereby the implant is formed in situ in the body of the mammal. A process for preparing a composition useful for biomedical application, comprising the steps of providing a liquid composition comprising an aqueous solution of dextran having a molecular weight of 1-100 kDa; and bringing the liquid composition to solidify; whereby water is gradually eliminated from the liquid composition during the solidification. A biomedical article prepared from the composition.
CN101139375A Synthesis of 1-hydrocarbyl-2-(4-beta-D-pyrane allose glycosides-phenyl)-benzimidazole derivative The present invention provides the synthesis method for 1 - alkyl 2 - (4 - Beta-D-glucoside alor - phenyl) - benzimidazole derivatives, and discloses a preparation method for bean-curd fruit derivatives that can improve the central nervous system. The compounds are of good sedative, hypnotic and anticonvulsant effects. At present, the product is included in the Chinese Pharmacopoeia of the 2000-year version under the name of ''Nervous-evoking Fruit Pill''. The bean-curd fruit derivative has the chemical formulas (I) and (II). The bean-curd fruit derivatives provided in the present invention are compounds which take plant active monomers bean-curd fruits that are of sedative, hypnotic and anticonvulsant effects as the matrixes. The structure of the present invention is improved and designed under the principles of drug structure molecular. The present invention is compound which can improve the central nervous system and is of high activity.
EP2606050A2 Heterocyclyl pyrazolopyrimidine analogues as selective jak inhibitors The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
CN101830897A Novel isoquinoline alkaloid derivatives and preparation method and application thereof The invention discloses tetrahydropalmatine derivatives and a preparation method and application thereof. The structural formula of the tetrahydropalmatine derivatives is shown as a formula II, wherein R is octyl, isopropyl or 3-methybutyl. The provided application is the application of the tetrahydropalmatine derivatives shown as the formula II or pharmaceutically acceptable salts thereof in the preparation of eukaryotic tumor cell antiblastics and medicaments for preventing and/or treating tumors. The results of in-vitro anti-tumor activity experiments prove that each tetrahydropalmatine derivative has the effect of inhibiting human lung cancer cells A-549, KB human nasopharyngeal carcinoma cells, and HL-60 leukemia cell strains to a certain extent. The results show that the tetrahydropalmatine derivatives shown as the formula II can be applied to preparing the medicaments for treating the tumors, and the pharmaceutical application of the tetrahydropalmatine derivatives is widened.
US20100249074 Benzyl-cycloalkyl sphingosine 1-phosphate receptor modulators Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.
US20070142400 Enantjomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl) sulfonyl] piperazine The invention provides a method for the treatment of allergic conditions by administering to a patient an effective amount of dextrorotatory dihydrochloride of 2-[2-[4-[(4-chloro-phenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid. The treatment is conducted in the absence of levorotatory dihydrochloride of 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid.
CN103655485A Alprostadil lipid microsphere preparation and preparing method thereof The invention discloses an alprostadil lipid microsphere preparation prepared from alprostadil and/or a salt thereof, oil for injection, an emulsifier, a co-emulsifier, an osmotic pressure regulator, a metal complexing agent, an antioxidant, a pH regulator and water for injection. The preparation comprises the components: 0.001-5 g/L of the alprostadil and/or the salt thereof, 50-500 g/L of the oil for injection, 6-36 g/L of the emulsifier, 0.1-5 g/L of the co-emulsifier, 10-30 g/L of the osmotic pressure regulator, 0.01-5 g/L of the metal complexing agent, and 0.01-30 g/L of the antioxidant, wherein the pH regulator is added until the pH value of the preparation is 5.5-6.0. The preparation is used for preparing alprostadil lipid microspheres, and the obtained product has the characteristics of high entrapment rate, good stability of emulsion particles, good preparation chemical stability and small drug administration stimulation, is convenient for administration and clinical application when being used in the alprostadil lipid microspheres, and can reduce costs and sterile risks.
EP1313462B1 Use of asiatic acid or asiaticoside for treatment of cancer Products containing asiatic acid or asiaticoside, and uses thereof, for the treatment of cancer and other proliferative diseases are provided.
EP1942909A2 Methods for treating respiratory disorders The invention provides methods for treating respiratory disorders in a patient in need thereof comprising administering an effective amount of (i) at least one hydralazine compound or a pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and/or isosorbide mononitrate, and (iii) optionally at least one therapeutic agent. The hydralazine compound may be hydralazine hydrochloride. The respiratory disorders may be chronic obstructive pulmonary disease, pulmonary hypertension, emphysema, asthma, cystic fibrosis and bronchitis.
CN101077349A Total alkaloids of subprostrate sophora root soft capsules and preparation method and application thereof The present invention discloses one kind of soft capsule of tonkin sophora root total alkaloid. The soft capsule consists of two parts, inclusion and covering. The inclusion includes Tonkin sophora root total alkaloid, dispersing medium and stabilizer; and the covering includes gelatin, glycerin, water and preservative. The present invention also discloses the preparation process. The preparation process is simple, and the soft capsule of tonkin sophora root total alkaloid has high stability, controllable quality, easy taking and high antitumor effect.
EP2751097A2 Processes for making compounds useful as inhibitors of atr kinase The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula (I) or (II) wherein the variables are as defined herein.
WO2008021932A3 Milnacipran for the treatment of cognitive dysfunction associated with fibromyalgia Methods for treating cognitive dysfunction associated with fibromyalgia by administering high-dose milnacipran to a patient suffering from such cognitive dysfunction are provided. Also provided are methods for the long-term treatment of cognitive dysfunction associate with FMS by administering milnacipran to a patient suffering from such cognitive dysfunction.
US20090131392 Phtalocyanine derivatives, process for their preparation, pharmaceutical compositions containing them and their use Phthalocyanine derivatives are described having photosensitising characteristics and high solubility in water, useful for photodynamic treatment of bacterial infections, in particular infections generated by Gram-negative bacteria.
US20100143440 Ul97 inhibitors for treatment of proliferative disorders Methods and compositions related to treating or preventing a proliferative disease in a subject comprising administering an inhibitor of a UL97 or a UL97 homolog to the subject are described.
CN103232348A Fibrate-natural antioxidant twin drug used for treating hyperlipidemia, and preparation method thereof The invention relates to a fibrate-natural antioxidant twin drug used for treating hyperlipidemia, and a preparation method thereof. The invention discloses a twin drug composed of fibrate or active metabolite thereof and a natural antioxidant. The invention also discloses a synthesis reaction thereof. The twin drug can be used in hyperlipidemia treatment. With the twin drug, adverse reactions before the two drugs are systematically combined are reduced, and pharmacological effects are enhanced, such that a synergetic treatment purpose is achieved.
CN101298466A Oleanolic acid derivate, preparation and use thereof The invention educes functional groups like carbonyl group, indole heterocycle, paradiazine heterocycle, quinoline heterocycle and phenyl hydrazone cycle, etc. in an A circle of a mother nucleus of an oleanolic acid; the obtained oleanolic acid derivatives can all be used for anti-osteoporosis drugs and healthy food; moreover, most of the derivatives have strong restraining function on the osteoblast differentiation caused by active vitamin D; the preparation method for oleanolic acid derivatives of the invention is clear and easy; moreover, the method is easy to control to generate the derivatives of various structures which can be used for the anti-osteoporosis drugs and healthy food and prepared into medicament forms like oral liquids, troches, and capsules, etc.
US20090076066 Deuterium-enriched zolpidem The present application describes deuterium-enriched zolpidem, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
WO2008088006A1 Ap2 inhibitor The object is to inhibit the phosphorylation activity of PKD and the transcription inhibition activity of AP2α with high efficiency and improve the efficiency of transcription of ABCA1 gene. Disclosed is an AP2 inhibitor comprising a doxazosin compound (e.g., doxazosin, a derivative thereof, or a (physiologically or pharmacologically acceptable) salt of doxazosin or the derivative). Preferably, the doxazosin compound is doxazosin mesilate or the like. The doxazosin compound can inhibit the phosphorylation activity of PKD and the transcription inhibition activity of AP2α with high efficiency, and can also promote the transcription of ABCA1 gene to thereby promote the production of an HDL. Thus, further disclosed are: a PKD inhibitor, an ABCA1 transcription promoter and an HDL production promoter, each comprising a doxazosin compound; and an ABCA1 transcription promoter and an HDL production promoter, each comprising the AP2 inhibitor or the PKD inhibitor.
US20100215659 Functionalized surgical adhesives A bioadherent composition includes a first mixture containing a plurality of reactive members of a specific binding pair, said reactive members being bound to a ligand capable of binding a receptor on biological tissue, and a second mixture containing a plurality of complementary reactive members of the specific binding pair, said complementary reactive members being bound to a ligand capable of binding a receptor on biological tissue, said reactive members capable of forming covalent bonds with said complementary reactive members via a reaction selected from Huisgen cycloaddition reactions, Diels-Alder reactions, and/or thiol-alkene reactions. A method for bonding biological tissue involves utilizing the bioadherent composition.
WO2011002100A1 Medicament for the long term nsaid use Provided is a medicament comprising cobiprostone or its pharmaceutically acceptable salt, ester, ether or amide for the long term treatment of a disease or condition which is one of indications for NSAID use in a human patient, wherein cobiprostone is administered at least 36 mcg per day to the patient who receives a NSAID. By administering cobiprostone or its pharmaceutically acceptable salt, ester, ether or amide in combination with a NSAID, the patient can receive the NSAID for longer time period.
US20110112058 Novel modulators of calcium release-activated calcium channel and methods for treatment of non-small cell lung cancer Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
US20090221611 Fused Triazole Tachykinin Receptor Antagonists The present invention is directed to certain fused triazole compounds which are useful as neurokinin-1 (NK-I) receptor antagonists, and inhibitors of tachykinin and in particular substance P- The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
US20090004309 Anti-Gastritis and Anti-Ulcer Agent Containing Momordicae Semen Extract and Momordica Saponin I Isolated From the Same The present invention relates to a Momordicae semen extract effective in the prevention and treatment of gastritis or gastric ulcer and momordica saponin I isolated therefrom. The Momordicae semen extract and the momordica saponin I isolated therefrom is effective in the prevention and treatment of gastritis or gastric ulcer since they prevent the damage of the gastric mucosa caused by alcohols and inhibit the secretion of gastric acid.
DE102005018026A1 New substituted styrol stereoisomers are glucocorticoid receptor ligands useful for the treatment of e.g. inflammatory diseases, lung diseases, rheumatic diseases, autoimmune diseases, joint disorders and gastrointestinal disorders Substituted styrol stereoisomers of formula (I) are new. Substituted styrol stereoisomers of formula (I) are new. Either R1>, R2>(1-10C)-alkyl, (1-10C)-alkoxy, (1-10C)-alkylthio, (1-5C)-perfluoroalkyl, (all optionally substituted), H, OH, halo, CN or NO2; or R1>R2>-O-(CH2)n-O-, -O-(CH2)n-CH2-, -O-CH=CH-, -(CH2)n+2-, -NH-(CH2)n+1, N(1-3C-alkyl)-(CH2)n+1, -NH-N=CH- (where terminal atoms are directly connected with adjacent ring carbon atoms) or NR9>R1>0>; or R1>R8>5-8 membered carbocycle- or heterocycle, optionally substituted by 1-2 of keto groups, (1-5C)-alkyl, (1-5C)-alkoxy or 1-4 of halo atoms; R9>, R1>0>H, (1-5C)-alkyl or (CO)-(1-5C)-alkyl; R4>(1-10C)-alkyl (optionally substituted with OH, halo or (1-5C)-alkoxy), (3-7C)-cycloalkyl, heterocyclyl, aryl or mono- or bicyclic heteroaryl, optionally substituted with (1-5C)-alkyl (optionally substituted with 1-3 of OH or COOR1>1>), (1-5C)-alkoxy, OH, halo or 1-2 of (1-3C)-exoalkylidene, containing 1-4 of N, 1-2 of O or S and/or 1-2 of keto groups, where these groups are connected over any position of the amine of the styrol systems, and optionally hydrated at one or more places; R1>1>(1-5C)-alkyl or benzyl; R5>(1-5C)-alkyl (partially or completely fluorinated), (3-7C)-cycloalkyl, (3-7C)-cycloalkyl-(1-8C)-alkyl, (3-7C)-cycloalkyl-(2-8C)-alkenyl, heterocyclyl, heterocyclyl-(1-8C)-alkyl, heterocyclyl-(2-8C)-alkenyl, aryl, aryl-(1-8C)-alkyl, aryl-(2-8C)-alkenyl, aryl-(2-8C)-alkynyl, mono- or bicyclic heteroaryl, optionally substituted with one or more keto groups, (1-5C)-alkyl, (1-5C)-alkoxy, halo or (1-3C)-exoalkylidene, containing 1-4 of N, 1-2 of O or S, where heteroaryl-(1-8C)-alkyl or heteroaryl-(2-8C)-alkenyl are connected over an any position of styrol system and optionally hydrated at one or more places; either R6>H, halo or (1-10C)-alkyl, optionally substituted by OR1>0>, SR1>0>, N(R1>0>R9>) or 1-3 of halo; or R7>H, halo, (1-10C)-alkyl (optionally substituted by OR1>0>, SR1>0> or N(R1>0>R9>) or CN; or R7>+C-atom of methyl : (3-6C)-cycloalkyl or (1-5C)-alkylidene; or R6>R7>5-8 membered carbocycle- or heterocycle, optionally substituted with 1-2 of keto groups, (1-5C)-alkyl, (1-5C)-alkoxy or 1-4 of halo); and n : 1 or 2. [Image] - ACTIVITY : Antiinflammatory; Respiratory-Gen.; Antiallergic; Antirheumatic; Immunosuppressive; Osteopathic; Antiarthritic; Antipyretic; Dermatological; Muscular-Gen.; Antipsoriatic; Nephrotropic; Hepatotropic; Gastrointestinal-Gen.; Ophthalmological; Neuroprotective; Antibacterial; Gynecological. - MECHANISM OF ACTION : Glucocorticoid receptor ligand.
CN102977116A Amorphous prasugrel hydrogen sulfate and preparation method thereof The invention relates to amorphous prasugrel hydrogen sulfate and a preparation method thereof. The preparation method comprises the steps of mixing prasugrel salt with an organic solvent, and controlling the temperature of the solution to be 0-30 DEG C; adding carbonate or hydrocarbonate water solution in the solution to react until the pH value of the system is 7-10; respectively collecting an organic phase and a water phase; evaporating the organic solvent in the organic phase to obtain the prasugrel; adding the organic solvent to the prasugrel, so that the prasugrel is completely dissolved; controlling the temperature of the solution to be 20-30 DEG C, dripping sulfuric acid solution, and then reducing the temperature of the system to -10 to 10 DEG C to obtain the amorphous prasugrel hydrogen sulfate. An X-ray powder diffraction spectrum, which is represented by a diffraction angle 2theta, of the product does not contain crystal form characteristic peaks; a detection of a differential scanning calorimeter indicates that no definite melting point exists; and the purity, the color and the shape of the product are not changed after the product is stored for 100 days at normal temperature under a drying condition, and commercial industrial large-scale implementation is more easier.
CN101530422A Liquid-phase adenosine triphosphate coupled nanometer simple substance selenium and preparation and storage method thereof The invention relates to nanometer selenium, and in particular discloses adenosine triphosphate coupled nanometer simple substance selenium and a preparation and storage method thereof. The preparation method comprises the following steps: at normal temperature and normal pressure, adding vitamin C solution to adenosine triphosphate solution; after mixing uniformly, dropping selenium dioxide or selenite solution, and uniformly mixing the solutions during dropping; and obtaining a liquid-phase coupling product formed by the adenosine triphosphate and the nanometer simple substance selenium. The method uses small molecule adenosine triphosphate with anti-cancer activity to carry out good grain diameter control and stabilization on the nanometer simple substance selenium to obtain the selenium form with high anti-cancer activity and low toxicity, and the obtained product can be stored in a liquid phase in the form of hydrosol so as to be favorable for the development of various dosage forms such as injections, oral agents, spraying agents, cream, and the like so as to greatly broaden the range of application.
EP2659894A1 Ophthalmic solution containing diquafosol, method for producing same, and method for preventing formation of insoluble precipitate Regarding Diquafosol ophthalmic solution comprising a chelating agent, formation of insoluble precipitates found in Diquafosol ophthalmic solution during its storage, as well as deterioration of the filtration performance in the course of production (filtration sterilization), have been inhibited. Further, in Diquafosol ophthalmic solution comprising a chelating agent, enhancement of preservative effectiveness has been confirmed. Accordingly, the present invention provides Diquafosol ophthalmic solution having physicochemical properties that are stable during the courses of production and distribution as well as the course of storage by a patient. Particularly in the course of production, the solution can be subjected to efficient filtration sterilization. Moreover, the solution has excellent preservative effectiveness. The present invention also provides a method for inhibiting formation of insoluble precipitates from an aqueous ophthalmic solution comprising diquafosol or a salt thereof, by adding a chelating agent to the solution.
CA2559510A1 Compositions and methods for reducing vaginal ph This invention relates to aqueous buffered compositions and methods for lowering vaginal pH and reducing the level of self perceived vaginal odor. Such compositions may be applied to the vaginal area to lower vaginal pH and assist in maintaining such pH over a period of time.
WO2007116916A1 Liquid drug preparation for oral administration [PROBLEMS] To provide a liquid drug preparation for oral preparation by which the labor at drug-taking can be saved to thereby reduce patient burden and which enables safe drug-taking. [MEANS FOR SOLVING PROBLEMS] A liquid drug preparation for oral preparation which is packaged in a container having a discharge unit and administered via direct discharge from the discharge unit onto the tongue or the vicinity thereof in the oral cavity without any contact.
CN101991571A Application of curcumin plus mitomycin C in preparing medicine used for treating breast cancer The invention discloses application of curcumin plus mitomycin C in preparing medicine used for treating breast cancer. Curcumin plus mitomycin C (MMC) is applied to in vitro human breast cancer cell model and in vivo xenotransplated tumour naked mouse model, the effects of attenuation and synergism are realized compared with the condition that MMC is independently applied; wherein medicine concentrations when in application of in vitro human breast cancer cell are as follows: curcumin: 40MuM; MMC: 2.5MuM; and MMC: 5MuM when being applied independently; and the medicine concentration when in application of in vivo xenotransplated tumour naked mouse are as follows: curcumin: 100mg/kg; MMC: 1-2mg/kg; and MMC: 1-2mg/kg when being applied independently. The invention adopts combination of curcumin and MMC to improve growth inhibition on cell and tumour, improve kidney function, reduce bone marrow suppression, promote cell apoptosis, induce cell cycle arrest and reduce DNA crosslinking angle of MMC, effects of attenuation and synergism on breast cancer treatment are realized compared with the condition that chemotherapy medicine MMC is applied independently, and principle thereof is clarified, thus laying the foundation for clinical medication.
US20110229550 Acid-Degradable and Bioerodible Modified Polyhydroxylated Materials Compositions and methods of making a modified polyhydroxylated polymer comprising a polyhydroxylated polymer having reversibly modified hydroxyl groups, whereby the hydroxyl groups are modified by an acid-catalyzed reaction between a polydroxylated polymer and a reagent such as acetals, aldehydes, vinyl ethers and ketones such that the modified polyhydroxylated polymers become insoluble in water but freely soluble in common organic solvents allowing for the facile preparation of acid-sensitive materials. Materials made from these polymers can be made to degrade in a pH-dependent manner. Both hydrophobic and hydrophilic cargoes were successfully loaded into particles made from the present polymers using single and double emulsion techniques, respectively. Due to its ease of preparation, processability, pH-sensitivity, and biocompatibility, of the present modified polyhydroxylated polymers should find use in numerous drug delivery applications.
CN103339103A [((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-acetic acid isopropyl ester and related compounds and their use in therapy The present invention pertains generally to the field of coolants and medical therapy. More particularly, the present invention relates to certain anti-nociceptive agents, such as [((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-acetic acid isopropyl ester, that are potent and long-acting and selectively cooling for non-keratinized epithelial tissues as compared to keratinized epithelial tissues, and are useful, for example, for the treatment of (e.g., the alleviation of symptoms of; the amelioration of) sensory discomfort of non-keratinized stratified epithelial (NKSE) tissue;and so for treatment of: sensory discomfort of an ocular surface, an eyelid, a margin of an eyelid, an anterior part of an eyeball, a conjunctiva, a lachrymal system, a pre-corneal film, or a cornea, a lining of the oral cavity, an internal portion of the lips, a pharyngeal surface, an esophageal surface, or an anogenital surface; eye discomfort, e.g., caused by extended wear of contact lenses, by eye strain and/or fatigue, by air pollutants, by excessive exposure to the sun, by conjunctivitis, by dry eye syndrome; sensory discomfort associated with oral mucositis; airway (e.g., larynx, trachea, and/or bronchi) tightness, discomfort in the airways (e.g., larynx, trachea, and/or bronchi), choking, cough, and/or dyspnea, e.g., associated with asthma and/or chronic obstructive pulmonary diseases (COPD).
US7074829 Antiestrogens, process for their production and their pharmaceutical use This invention relates to new antiestrogens of the general formula in which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens). Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.
CN101297806B Novel use of adenylate activated protein kinase inhibitor Compound C The invention discloses an application of an AMP-activated protein kinase (AMPK) inhibitor compound C in the preparation of drugs for prevention and treatment for obesity. The AMPK activity inhibitor compound C can inhibit a differentiation process to fat cells of pre-fat cells. The compound C not only can inhibit the AMPK activity, but also can carry out dose-dependent inhibition of lipid formation, decrease the expression level of key transcription factor C/EBP family and PPAR Gamma in an early stage of differentiation of the pre-fat cells and inhibit the cloning proliferation process in the early stage of differentiation of the pre-fat cells during the differentiation process of the 3T3-L1 pre-fat cells. The new application of the AMPK inhibitor compound C of the invention provides a new drug for clinical prevention and treatment for obesity.
CN101230049A Hydroxamic acid histone deacetylase inhibitor as well as preparation method and use thereof The invention relates to a hydroxamic acid histon deacetylase inhibitor (I), discloses the preparation method of a compound, the medical preparation containing the compound and the medical use thereof, and belongs to the pharmaceutical chemistry field.
CN102920718A Application of phenylethanoid glycoside monomeric compound The invention relates to the field of medicines and discloses an application of a phenylethanoid glycoside monomeric compound savatiside A in preparation of a medicament used for preventing and treating infectious diseases caused by pathogenic microorganisms. According to the invention, an inhibition zone test is carried out through a diffusion method, and the minimal inhibitory concentration and the minimum bactericidal concentration of savatiside A are measured through a microporous dilution method, so as to prove that savatiside A has bacteriostatic and bactericidal effects. Furthermore, savatiside A is proved to have an obvious protective effect on bacterial infection through functions of savatiside A on ichorrhemia resulting from mice systemic infection caused by a mixed bacteria liquid of pseudomonas aeruginosa, colon bacillus, bacillus subtilis and staphylococcus aureus. Moreover, savatiside A is proved to have obvious intracorporal bacteriostatic and bactericidal effects through a staphylococcus aureus pneumonia model and a pseudomonas aeruginosa pneumonia model.
CA2163793C Novel antiviral agents Novel antiviral (including antiretroviral) compounds are mono- or dicarboxylic acid esters of bypericin in which one or both of the methyl groups of hypericin are substituted by carboxylic acid ester groups of the formula COOR3 in which R3 is alkyl, the chain of which is optionally interrupted by one or more oxygen or sulphur atoms. R3 is preferably methyl, ethyl, propyl, butyl, 2-methoxyethyl or 2-(2-methoxyethoxy)ethyl. The compounds may be formulated into pharmaceutical compositions and may be used in any manner which has previously been known for hypericin.
WO2007093873A1 Bis-pyrr0l0[2,l-c] [1, 4] benzodiazepine- anthraquinone conjugates as antitumour agents and a process for the preparation thereof The present invention provides novel bis-pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone conjugates of general formula (V), useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of novel bis-pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone conjugates of general formula (V),wherein n=3, 4 or 5.
EP1789405A1 Novel enantiomerically pure beta-agonists, method for the production and the use thereof in the form of a drug The invention relates to enantiomerically pure compounds of formula (1), wherein the radicals R1, R2, R3, R4 and X are defined as in claims and a description. A method for producing said compounds and the use thereof in the form of a drug, in particular as a drug for treating respiratory tract diseases are also disclosed. The synthesis of the compounds is carried out by means of a chiral epoxide of formula (5).
CA2493831A1 Amino acid esters as nutrient supplements and methods of use The present invention provides novel nutrient and food supplement amino acid ester compounds and compositions for human and animal consumption.
CN103040722A Hydrochloride thiamphenicol glycinate lipidosome injection The invention discloses a hydrochloride thiamphenicol glycinate lipidosome injection and a preparation method thereof. The lipidosome injection is prepared by using hydrochloride thiamphenicol glycinate, egg yolk lecithin, soybean phospholipid phosphatidyl inositol, soyasterol and lactose according to a specific weight ratio. The hydrochloride thiamphenicol glycinate lipidosome injection disclosed by the invention has the advantage of good preparation stability; after the hydrochloride thiamphenicol glycinate lipidosome injection is stored for a long time, a lipidosome is also kept with good encapsulation efficiency; the quality of a preparation product is improved, the retention time of a drug in systemic circulation is prolonged, the biological availability of the drug is increased, toxic and side effects are reduced and a curative effect is obviously improved; and moreover, the hydrochloride thiamphenicol glycinate lipidosome injection disclosed by the invention has the advantage of simple preparation method and is suitable for large-scale industrial production.
CN102091041A Novel nanoparticle of camptothecin drug and preparation method thereof The invention provides a nanoparticle of an insoluble anti-tumor drug such as camptothecin and its derivatives (CPTs) as well as a preparation method thereof. The nanoparticle of the camptothecin has an average diameter of 10-500 nanometers and good water dispersity and can stably exist in simulated body fluids and enhance the cell killing effect by 4-5 times. The preparation method disclosed by the invention can be implemented by only mixing two solutions and carrying out centrifugal washing and has simple step and good repeatability and is easy to realize industrial expansion.
US20120040946 Medicinal fusidic acid cream made using sodium fusidate and incorporating a biopolymer and a process to make it The present invention is directed to a medicinal composition for treating bacterial skin infections and related wounds, and also other skin wounds including those caused by burns. The cream also causes skin rejuvenation through an epithelisation process. The cream comprises a) a biopolymer in the form of Chitosan, b) an Active Pharmaceutical Ingredient (API), in the form of fusidic, c) a cream base, and d) water. The invention also discloses a process to make the medicinal cream in which Fusidic acid which is formed in situ from Sodium Fusidate as the starting raw material, by converting it into Fusidic acid under oxygen-free environment created using inert gas, preferably nitrogen. The cream produced by the process of the present invention has greater shelf-life stability and the finer particle size of the API than the conventional creams containing Fusidic acid and found to be surprisingly superior for use against skin infections with allergy & itching, & wounds on human skin than alternative creams currently available.
CN101516366B Oxindole derivatives as anticancer agents There is provided compounds of the formula (I) wherein R<6>, V, W, X, Y and n are as described. The compounds exhibit activity as anticancer agents.
WO2007148804A1 Composition capable of promoting the production of hyaluronic acid Disclosed is a novel composition capable of remarkably promoting the production of hyaluronic acid. The composition comprises (A) at least one member selected from the group consisting of retinol and a derivative thereof and (B) at least one member selected from the group consisting of a peptide represented by Leu-Glu-His-Ala (Formula I), a derivative thereof and a salt of the peptide or the derivative. Alternatively, the composition comprises (A) at least one member selected from the group consisting of retinol and a derivative thereof and (B) at least one member selected from the group consisting of a peptide having the conservative substitution, deletion and/or addition of at least one amino acid residue in the amino acid sequence: Leu-Glu-His-Ala (Formula I) and capable of promoting the production of hyaluronic acid in a cell, a derivative thereof and a salt of the peptide or the derivative.
US20060270728 Substituted dihydropyrano indole-3,4-dione derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
CN101693670A Benzoic acid nitrogen mustard derivative as well as preparation method and application thereof The invention relates to a benzoic acid nitrogen mustard derivative which has the following formula: R1 is 4-CH3-C6H5, 4-CH3O-C6H5, 4-CH(CH3)2-C6H5, 4-F-C6H5, 4-Cl-C6H5, 4-Br-C6H5, 4-NO2-C6H5, 2-F-C6H5, 2-Cl-C6H5, 2-Br-C6H5, n-butyl, tertiary butyl and n-dodecyl, and R2 is H; or R1 is CH3-, and R2 is C6H5-; or R1 and R2 are both n-propyl and n-butyl. The benzoic acid nitrogen mustard derivative has remarkable inhibiting effect for human oral cavity epicuticula cancer cell strain (KB) and human leukaemia cell strain (K562) so that the benzoic acid nitrogen mustard derivative can be applied in preparing antitumor medicaments. The invention also discloses a preparation method of the benzoic acid nitrogen mustard derivative.
WO2010013158A1 Phenanthrenone compounds, compositions and methods The present invention is directed to compounds of Formula (I) or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
WO2009087602A1 Compositions for use in the treatment and prevention of ulcerative collitis The invention provides compositions and methods for treating and preventing ulcerative colitis. The compositions and methods of the invention are based on a novel use of thiocyanate or isothiocyanate comprising compounds and other compounds useful for enhancing thiocyanate or isothiocyanate levels in the serum and/or in the colon.
CN103006623A Application of mannitol in preparation of anti-stomach cancer drug The invention discloses an application of mannitol in preparation of an anti-stomach cancer drug, and in particular relates to a use of a mannitol injection with a specific concentration of 10%-19% for treating stomach cancer. Traditionally, mannitol is only used as a diuretic, a high-permeability hypotensor and the like, while the inventor discovers through scientific experiments that mannitol has anti-tumor activity, and through several cell apoptosis detection technologies and by detecting apoptosis-related genes bcl-2, and bax, proves that the specific-concentration mannitol can induce various human cancer cell strains to generate obvious cancer cell apoptosis, grasps the effect relation with concentration and time, and first illustrates the possible mechanism; furthermore, the inventor has used the research result for tumor patient treatment and has achieved obvious curative effect, which provides theoretical basis and practical cases for the application of mannitol in the preparation of the anti-tumor drug and the clinical generalization thereof.
US20110123452 Metal oligomers and polymers and their use in biology and medicine Described herein are a class of metal oligomers and polymers that contain both metals and organic groups. Said oligomers and polymers have utility in many applications including biomedical imaging, radiation therapy, drug delivery, and in vitro analytical techniques, such as fluorescence and phosphorescence.
CN102008582A Angelica sinensis chengqi decoction and application thereof The invention relates to an angelica sinensis chengqi decoction which is prepared from the following bulk pharmaceutical chemicals in parts by weight: 400-800 parts of rheum officinale, 200-400 parts of mirabilite, 400-800 parts of angelica sinensis, 200-300 parts of pericarpium citri reticulatae, 140-180 parts of snakegourd seed, 60-100 parts of snakegourd peel, and 1-2 parts of ethylparaben. The invention also provides application of the angelica sinensis chengqi decoction in preparing a medicine for treating an excited disquieting disease, a conduct disorder disease and an abdomen distension and constipation. The decoction provided by the invention has the advantages that the bulk pharmaceutical chemicals required by the medicine are less and are easy to obtain; the medicine can be prepared conveniently and the operation is simple; and the decoction has characteristics of rapid and obvious curative effect and few side effects, and is suitable for clinical practice.
US8828974 Substituted propane phosphinic acid derivatives The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
CN1634025A Use of erberry and its lignanoids compound in drug for osteoporosis The invention relates to the use of Sambucus Williamsii Hance as osteoporosis resisting medicament, and the use of lignan compounds and phenolic acid compounds as osteoporosis resisting medicament, wherein the lignan compounds and phenolic acid compounds are prepared through the steps of ethanol heating backflow of Sambucus Williamsii Hance stems and branches, extracting ethanol extract, suspending in water and extracting with chloroform, acetic acid ethyl ester, and n-butyl alcohol, disintegrating with chemical means. The invention shows no side action of estrogen samples.
CN101703580A Externally used medicinal preparation for detumescence and analgesia and preparation method thereof The invention discloses an externally used medicinal preparation for detumescence and analgesia and a preparation method thereof. The externally used medicinal preparation is prepared from giant knotweed rhizome, gypsum ustum, borneol, ground sesameseed oil and hard paraffin. Compared with the prior art, the medicinal preparation is safe and effective and has stable properties, a simple preparation process and low-price and readily-available basic remedy raw materials. Years of clinical verification show that the medicinal preparation does not have adverse reaction and toxic and side effects, and when the medicinal preparation is used for treating parotitis through external application, the total clinical effective rate for treating the parotitis reaches 89.6 percent.
EP1905831A2 Lactoferrin receptor genes of moraxella Purified and isolated nucleic acid molecules are provided which encode lactoferrin receptor proteins of Moraxella, such as M. catarrhalis, or a fragment or an analog of the lactoferrin receptor protein. The nucleic acid sequence may be used to produce recombinant lactoferrin receptor proteins Lbp1, Lbp2 or ORF3 of the strain of Moraxella free of other proteins of the Moraxella strain for purposes of diagnostics and medical treatment. Furthermore, the nucleic acid molecule may be used in the diagnosis of infection.
EP1423147B1 Prostaglandin compositions and methods of treatment for male erectile dysfunction The invention provides methods and compositions for treating erectile dysfunction. The methods include the step of placing within the fossa navicularis of the patient an effective erection-inducing amount of a vasoactive prostaglandin composition of a semi-solid consistency. The composition comprises a vasoactive prostaglandin, a penetration enhancer, a shear-thinning polysaccharide, a lipophilic compound, and an acidic buffer system. The penetration enhancer is an alkyl-2-(N-substituted amino)-alkanoate ester, a (N-substituted amino)-alkanol alkanoate, or a mixture of these enhancers. The lipophilic compound may be an aliphatic C1 to C8 alcohol, aliphatic C2 to C30 ester, an aliphatic C8 to C30 ester, or a mixture of these. The composition includes a buffersystem providing a buffered pH value for said composition in the range of about 3 to about 7.4.
EP2123285A1 Nucleosidic phosphoantigens for use in VGAMMA9DELTA2 T cell-mediated therapy The present invention relates to nucleosidic phosphoantigens for the treatment of the human or animal body by therapy. The invention also relates to a method for stimulating Vγ9Vδ2 T cell-mediated immune response, which comprises the step of administering to a subject in need thereof a therapeutically effective amount of nucleosidic phosphoantigens.
US20100144743 Compositions and methods for inhibition of tyrosine kinases Compositions for inhibiting the catalytic activity of tyrosine kinases comprising compounds represented by Formulas (I), (II), and (III). Methods for treating proliferative diseases comprising administering a therapeutically effective amount of the above compositions.
CN101342267B Donkey-hide gelatin angelica polymorpha & hoantchy particle and method of preparing the same The present invention relates to health food, ass-skin glue angelica stilbene particles which can improve the nutritional anemia, and a production method thereof. The active ingredients consist of rawmaterials which have the following weight ratio: 30 to 80 portions of ass-skin glue, 20 to 50 portion of angelica, 10 to 40 portions of prepared rhizome of rehmannia, 20 to 40 portions of radix astragali, 20 to 40 portions of Astraolylis lancea formalyrata, 1 to 4 portions of vitamin, 0.5 to 2 portions of ferrous lactate, and 750 to 1,000 portions of white sugar. The particles are molten by the ass-skin glue, extracted by the angelica, the prepared rhizome of rehmannia, the radix astragali and the Astraolylis lancea formalyrata, concentrated under the vacuum condition, deposited by alcohol which is then recycled, mixed, granulated, dried, cleaned, packaged, and processed with other technologies. The production method has the characteristics of scientific formula, reasonable process and soon. The trial on the human body has proven that the particles have the health function of improving the nutritional anemia, no adverse effects on health, but secure and reliable edible effects.
US7196109 Piperidine-1-carboxylic acid (6,7-difluoro-5-phenyl-1H-indazol-3-yl)amide; especially for treating neurodegenerative diseases; kinase inhibitor The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovaries syndrome, syndrome X, immunodeficiency and cancer.
WO2014140402A1 Use of derivatives with c-o-p bonds in patients with renal failure The invention relates to the use of a derivative with C-O-P bonds in the form of controlled release for the treatment of patients with renal failure. The invention also relates to the use of said derived compounds together with other active substances, that can particularly be selected from the list comprising a calcimimetic, a vitamin, a phosphorus chelator, thiosulfate, biphosphonate, pyrophosphate, citrate, a diuretic, an antihypertensive and an anticholesterolemic agent.
CN101822622A Preparation method and application of nano-citrulline gel The invention relates to a preparation method and the application of nano-citrulline gel. Citrulline comprises the following raw material components in parts by weight: 1 to 20 parts of citrulline, 1 to 20 parts of menthol, 0.5 to 20 parts of peppermint oil, 0.5 to 20 parts of peach oil, 0.25 to 15 parts of carbomer 934 type, 0 to 20 parts of vitamin E, 0 to 20 parts of vitamin B, 0 to 20 parts of collagen, 0 to 5 parts of coenzyme Q10, an appropriate amount of sodium hydroxide solution, and 0.5 to 80 parts of water. The product is obtained through the weighing, the dissolution, the mixing, the neutralization, the filling and other steps of all the raw material components. The product can be respectively prepared into four series of products, i.e. beauty nutrition gel for women, anti-prostate cancer and cervical gel for men and women, treatment assistant ED gel for men, child metabolic disorder treatment assistant and common nutrition gel, according the different combinations of citrulline and other auxiliary components, and has the advantages of simple production, low cost, and convenient and safety storage, carrying and use.
CN101712633A Alpha or beta-aldehyde ketone derivative, method for preparing same and activities thereof for resisting drug-resistance bacterium pathogens and helicobacter pylori The invention provides an alpha or beta-aldehyde ketone derivative with a structural formula (I) and a method for preparing the same. The alpha or beta-aldehyde ketone derivative possesses the activities for resisting drug-resistance bacterium pathogens and helicobacter pylori, and can be used in the preparation of medicaments for resisting drug-resistance bacteria.
US6962937 Imidazolidine derivatives, their preparation and their use The present invention relates to novel imidazolidine derivatives of the formula I, in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings given herein. The compounds of the formula I are valuable pharmaceutically active compounds which are suitable, for example, for treating inflammatory diseases, for example, rheumatoid arthritis, or allergic diseases. The compounds of the formula I are inhibitors of the adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4, which belongs to the integrin group. They are generally suitable for treating diseases which are caused by, or associated with, an undesirable degree of leukocyte adhesion and/or leukocyte migration or in which cell-cell or cell-matrix interactions, which are based on the interactions of VLA-4 receptors with their ligands, play a role. The invention furthermore relates to processes for preparing the compounds of the formula I, to their use and to pharmaceutical preparations which comprise compounds of the formula I.
WO2006066899A1 Novel thrombin inhibitors The invention relates to compounds of formula (I) wherein A, B, R1, R2, G, R3, D and E have the meaning as cited in the description and the 10 claims. Said compounds are useful as coagulants. The invention also relates to the production and use thereof as medicament.
CN102218028A Antisense oligonucleotide injection for treating liver cancer and preparation method thereof The purpose of the invention is to provide an injection preparation for liver cancer resistance with an antisense oligonucleotide drug Aitaide (which has a sequence of 5'-ACT CAC TCA GGC CTC AGA CT-3') as an active component, and a preparation method thereof. The injection comprises a lyophilized powder injection or a concentrated solution for preparing a solution before clinical intravenous drip, is prepared by the single-dose active component Aitaide and pharmaceutically effective additives, has a pH of 7-9, a content specification of 10 mg-500 mg; the pharmaceutically effective additives comprise 0-5% of antioxidants, 0-60% of fillers, 0-10% of stabilizers, 0-10% of pH regulators, and 0-10% of ionic strength regulators, and the above percentages are the percentage ratios of the total component mass to the solution volume. The antisense oligodeoxynucleotide injection for treating liver cancer of the invention has good inhibition effect on hepatoma cells, controllable quality, and good stability.
WO2009081107A1 P-menthawe-3-carboxylic acid esters to treat airways diseases The present invention relates to methods and devices for treating sensory discomfort in the upper airways of a human; treating sensory discomfort in the oropharynx of a human; alleviating pain from pharyngitis in a human; alleviating cough in a human; and ameliorating the symptoms and signs of asthma, dyspnea, sleep apnea, snoring, or chronic obstructive pulmonary disease in a human. According to the invention, an active compound is delivered, preferably selectively delivered, to the oropharynx, preferably the oropharyngeal surfaces, more preferably the lower retropalatal oropharynx (LRO) of the patient. According to the invention, the active compound is a compound of the following formula, wherein -R is C2 to C4 hydroxyalkyl or polyhydroxyalkyl.
EP1680112B1 N-(5-adamantane-1-yl-methoxy-pentyl)deoxynojirimycin or a pharmaceutically salt thereof for use in the treatment of insulin resistance The invention relates to the use of a deoxynojirimycin derivative, or pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of insulin resistance, hyperpigmentation and/or inflammatory processes in the skin, a fungal disease, overweight and obesity, or a microbacterial infection.
US20090202588 Nucleic acids encoding TGEV and PRRSV sequences for improved expression of PRRSV sequences The present invention relates to nucleic acids comprising: (a) sequences of a replication competent transmissible gastroenteritis virus (TGEV), which sequences encode a TGEV replicase under the control of expression regulatory sequences, wherein the replicase is expressed in a host cell and will initiate replication of the nucleic acid and thus increase the number of nucleic acids in the cell; and (b) a sequence encoding at least one neutralizing epitope of ORF5 of porcine reproductive and respiratory syndrome virus (PRRSV), which sequence includes a disulfide bridge forming residue; and (c) a sequence encoding at least one further polypeptide capable of increasing an immune response against PRRSV. The present invention further relates to vectors, virus particles and host cells comprising these nucleic acids as well as their use for the preparation of vaccines, specifically for the preparation of vaccines.
US20110044973 Treatment of cystic disease with lysophosphatidic acid antagonists A method for treating cystic diseases is disclosed herein. The method comprises administering lysophosphatidic acid receptor antagonists.
WO2009133686A1 Medicaments for treating alzheimer's disease Disclosed are novel medicaments used in the treatment or prevention of degenerative neurological disorders such as Alzheimer's disease. These are medicaments for treating Alzheimer's disease, and are also medicaments which prevent neuritic atrophy induced by amyloid β, in which a compound represented by formula (1) isolated from the flowers of the rose Rosa damascena is the active ingredient. Moreover, these are medicaments and medicaments for treating Alzheimer's disease, and are also medicaments which prevent neuritic atrophy induced by amyloid β, in which a straight long chain fatty acid is the active ingredient.
WO2005021008A1 Iontophoresis-administered composition An iontophoresis-administered composition comprising a water-soluble steroid stabilized in a water-containing iontophoresis-administered solution or gel composition, which iontophoresis-administered composition can realize absorption equal to or higher than that exhibited when a water-soluble steroid is administered in the form of an aqueous solution not mixed with any stabilizer. This iontophoresis-administered composition contains a water-soluble steroid and an edetic acid compound. This iontophoresis-administered composition can further contain at least one member selected from the group consisting of sugars, urea, surfactants and polyhydric alcohols.
CN101732277A Stable sitafloxacin medicinal composition and preparation method thereof The invention relates to a stable medicinal composition of sitafloxacin or salt thereof or a hydrate thereof and a preparation method. The composition contains the sitafloxacin or the salt thereof or the hydrate thereof and a medicinal pharmaceutical adjunct, wherein the medicinal pharmaceutical adjunct contains a diluting agent, a disintegrating agent, a lubricant and a powder coating material containing an opacifier. The preparation method of the composition is characterized by comprising the following steps: firstly, adopting a powder coating technology to carry out powder coating on the raw materials and part of the auxiliary materials and then carrying out the next preparation process. The opportunities that the raw materials contact with light are reduced after coating processing, thereby reducing the generation of a photodegradation product and enhancing the stability of the preparation greatly.
US6846953 Treating central nervous system disorders such as pain, depression, anxiety, schizophrenia, Huntington's disease, Alzheimer's disease or amyotrophic lateral sclerosis Aromatic and heteroaromatic amides of the formula where R1, R2 and R3 can be alkyl, X is alkylene, and R4 is an unsubstituted or substituted aromatic or heteroaromatic group such as naphthyl or fluorenyl, are CNS agents useful for treating pain, depression, anxiety, seizures, and schizophrenia.
CN102861042A Novel application of catalpol The invention discloses a novel application of catalpol, which belongs to the medicine technical field. The invention concretely relates to the application of catalpol in the preparation of medicines for treating cerebral arterial thrombosis sequelae, and the application of the catalpol in the preparation of medicines for promoting recovery of touch neurologic function of cerebral arterial thrombosis sequelae.
CN102133391A Autoserum compound for nourishing skin mesoderm and preparation method thereof The invention discloses an autoserum compound for nourishing the skin mesoderm and a preparation method thereof. The autoserum compound for nourishing the skin mesoderm is characterized by comprising the following raw materials in percentage by weight: 65-80% of fresh sterile autoserum, 15-30% of sterile phosphate buffered normal saline injection of which the concentration is 0.1mol/L and the pH is 7.2, 0.05-0.15% of sterile rh-bFGF (recombinant human basic fibroblast growth factor) freeze-dried powder, 0.05-0.20% of medicinal glycerol, 0.1-0.3% of medicinal mannitol and 0.1-0.3% of medicinal glycine. Compared with the commonly used autoserum, under the same effect, the autoserum compound disclosed by the invention has the advantage of less actual dosage, can be better cultured in the body tissue and filled into the skin pit, and has a very ideal effect on eliminating wrinkles. The autoserum compound disclosed by the invention has simple preparation processes, is easy in actual operation, has no need of special instruments, and is convenient to use.
EP2734516A1 Arylpyrazole ethers as inhibitors of leukotriene a4 hydrolase The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein A1, A2, A3, L1, L2 and D are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
WO2006122154A2 Pyridone derivatives for modulating stress-activated protein kinase system Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
WO2007018147A1 Pharmaceutical titanium dioxide composite material of which pharmacological effect can be eliminated by light irradiation Disclosed is a titanium dioxide composite material which can be dispersed in an aqueous solvent stably and can be administered to a living body in a simple manner and in which the pharmacological effect of a therapeutic compound carried on the composite material can be eliminated by irradiation with light. Also disclosed is a dispersion product of the composite material. The composite material comprises titanium dioxide which has a photocatalytic activity and a therapeutic compound attached to the titanium dioxide through a hydrophilic polymer. The composite material is stable in an aqueous solvent and can be administered to a living body in a simple manner. After the composite material is administered to a living body, a site on the living body where the pharmacological effect of the therapeutic compound is not needed to be developed can be irradiated with light to induce the light excitation of titanium dioxide at the site, thereby decomposing the therapeutic compound to reduce any adverse side effect of the therapeutic compound.
EP1778657A1 Fluorination process of protected aminothiazole A process for the production of fluorinated compound formula (I) comprising fluorination of a protected aminothiazole. Compounds formula (I) are useful in the preparation of activators of glucokinase.
WO2011123719A3 Use of faah inhibitors for treating abdominal, visceral and pelvic pain The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors alone or in combination for the treatment or prevention of abdominal, visceral or pelvic pain. Also described herein are pharmaceutical compositions comprising a FAAH inhibitor, alone or in combination with an additional therapeutic agent for the treatment of abdominal, visceral or pelvic pain.
US8506945 Polymers with structure-defined functions An alternating copolymer comprising a backbone of residues of a maleic anhydride derivative and those of a compound containing vinylic unsaturation, which also comprises residues of an active compound containing a nucleophilic group, bound to the backbone by a residue of the nucleophilic group, including such a copolymer comprising residues of an active compound containing an alcohol, thiol or amine group. The chemical and biological properties of actives, such as protease inhibitors, neurotransmitter drugs, and other small molecule active drugs, are enhanced, and new applications enabled. Also, artefacts, including a solid medical implant device, dressing or scaffold or a fluid adhesive or medicinal composition comprising such a polymer, and a method of use of such a polymer, including a method for the treatment or prophylaxis of wounds.
US20130158129 Natural, multiple release and re-use compositions A composition comprising a biopolymer matrix, said biopolymer matrix comprising from about 0.1% to about 40% of an essential oil, about 30% to about 95% of a biopolymer, and about 0% to about 50% of a carrier fluid wherein a limited amount of said essential oil can be released from said matrix composition when exposed to a liquid solution; and wherein an additional limited amount of said essential oil can be re-released repetitiously thereafter upon re-use with an additional exposure of a liquid solution.
CN103041403A Glucan-containing pharmaceutical composition and preparation method thereof The invention discloses a glucan-containing pharmaceutical composition which comprises glucan-polyethyleneimine and a pharmaceutically active component activated by cis-aconitic acid anhydride. Glucan and polyethyleneimine are bonded through urethane bonds, cis-aconitic acid anhydride and the pharmaceutically active component are bonded through amide bonds, and the pharmaceutically active component activated by cis-aconitic acid anhydride and glucan-polyethyleneimine are bonded through amide bonds which are jointed between cis-aconitic acid anhydride and polyethyleneimine. After entering a human body, the glucan-containing pharmaceutical composition forms a shell-core structure, can not be identified by the reticuloendothelial system, and gradually concentrates at the site of a tumor mass. Under the acidic conditions of the tumor site, the amide bonds between the pharmaceutically active component activated by cis-aconitic acid anhydride and polyethyleneimine are broken to release a large amount of the pharmaceutically active component, while the release of the pharmaceutically active component at other sites is extremely low, thus, the toxicity to the health cells is reduced, and the toxic or side effect is reduced. The invention discloses a preparation method of the glucan-containing pharmaceutical composition mentioned above.
EP1765779A1 New substituted piperidines as modulators of dopamine neurotransmission The present invention relates to compounds having therapeutic effects against disorders in the central nervous system, and in particular substituted hydroxypiperidines of the formula 1: wherein R1, R2, and R3 are as defined herein.
US20090018096 Methods For Regulating The Growth And/Or Survival Of Tumor Cells And Stem Cells By Modulating The Expression Or Function Of The Transcription Factor ATF5 The present invention provides methods for regulating the growth and/or survival of tumor cells and stem cells by modulating the expression or function of ATF5. The present invention also provides methods for promoting or suppressing differentiation of stem/progenitor cells, for producing differentiated cells and for isolating/purifying differentiated cells, including neural cells. Also provided are differentiated cells, cell populations and transgenic animals comprising same and uses of same. The present invention further provides methods for treating nervous tissue degeneration and for identifying an agent for use in treating nervous tissue degeneration. Methods for promoting apoptosis in neoplastic cells and for treating or preventing tumors, and identifying agents for use in treating or preventing tumors are also provided by the present invention. The present invention further provides methods for identifying agents that inhibit ATF5, agents identified by these methods. Also provided are methods for diagnosing tumors, for assessing the efficacy of therapy to treat tumors and for assessing the prognosis of a subject who has a neural tumor. Finally, the present invention provides a kits for use in detecting and treating tumors.
US20080227831 Contains N-methylnicotinamide; seaweed extracts; atherosclerosis The present invention is directed to N-methylnicotinamide containing food extracts, and their use in treating lipoprotein abnormalities and skin diseases and disorders.
US20050038062 Methods and materials for the treatment of pain comprising opioid antagonists Methods and compositions for treating subjects with pain, including neuropathic pain, using opioid antagonists or combinations of opioid antagonists and opioid agonists, including, for example, wherein the amount of an opioid antagonist enhances the neuropathic pain-alleviating potency of an opioid agonist.
CN201079620Y Medicament controlled-release catheter The utility model discloses a drug controlled release catheter which comprises an insertion end inserted into a body and a urine discharge end exposed outside the body. A catheterization opening of the insertion end is communicated with a urine-discharging opening of the urine-discharging end to for a catheterization channel. The utility model is characterized in that drug-releasing holes are arranged on the wall of the part of the insertion end which is positioned in a urethra, a drug supply tube is arranged at the urine-discharging end which is communicated with the drug-releasing holes through a drug-supply channel, and the drug-releasing holes and the drug supply channel are separated from the catheterization channel. Being provided with the drug-releasing holes and the drug supply tube, rapamycin or other drugs can be released through the drug supply tube and the drug-releasing holes, to prevent urethra from narrowing or recrudescence. The released amount and releasing time of the drugs can be controlled conveniently according to needs in this way.
EP1846410B1 Dihydroquinazolinones as 5ht modulators The present application provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
US7022687 for treatment of allergies and airway disorders such as allergic rhinitis The present invention relates to a novel combination of a soft steroid, in particular loteprednol, and at least one antihistamine, such as, for example, azelastine and/or levocabastine, for simultaneous, sequential or separate administration in the local treatment of allergies and airway disorders, for example of allergic rhinitis (rhinoconjunctivitis).
WO2005107731A1 Remedies containing vitamin k2 as the active ingredient NF-κB activation inhibitors and IκB phosphorylation inhibitors, containing vitamin K2 or hydrates thereof as the active ingredient. The invention brings about not only the efficacy of vitamin K2 as the remedy for a patient with liver cancer but also extremely high safeness in long-term administration of vitamin K2, which enables long-term treatment with vitamin K2 and contributes to great improvement in the quality of life of a patient with liver cancer.
WO2007124322A1 Inhibitors of c-fms kinase The invention is directed to compounds of Formula (I): wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula (I), are also provided.
US20090197832 Polymer mixtures of anionic and cationic polysaccharides and use thereof Described in the present application are compositions comprising mixtures of polyanionic polysaccharides and polycationic polysaccharides consisting of oligosaccharide derivatives of chitosan. In the compositions of the invention said mixtures have proven to be soluble in aqueous environments, despite ionic complexes forming between the acid polysaccharides and chitosan derivatives. Said compositions have also demonstrated significant rheological behaviour with an unexpected increase in viscosity and viscoelasticity, although the polysaccharides used have relatively low average molecular weights. The said solubility and rheological behaviour renders the compositions of the invention particularly advantageous from the biomedical application viewpoint, in particular for viscosupplementation and particularly in the field of articular pathologies and of ophthalmic surgery.
US20120202777 C-Linked Hydroxamic Acid Derivatives Useful As Antibacterial Agents The present invention is directed to a new class of hydroxamic acid derivatives of Formula I, wherein the variables G, T, D, L, A, X, R1 and R2 are as described hereinabove, and their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
US20110288086 Polycyclic quinazolines, preparation thereof, and use thereof At least one active pharmaceutical ingredient is chosen from polycyclic quinazolines of formula V, pharmaceutically acceptable salts thereof, and hydrates of the pharmaceutically acceptable salts. The active pharmaceutical ingredients disclosed may be inhibitors of protein tyrosine kinase inhibitors and/or aurora kinase. The active pharmaceutical ingredients can be used for treating cancers susceptible to treatment with protein tyrosine kinase inhibitors and/or aurora kinase inhibitors.
WO2010117829A3 Differentially expressed micrornas as biomarkers for the diagnosis and treatment of sjögren's syndrome The identification of differentially expressed microRNAs in patients with Sjögren's syndrome is disclosed herein. Provided is a method of diagnosing a subject as having Sjögren's syndrome by measuring the level of at least one differentially expressed miR gene product identified herein. An alteration in the level of the at least one miR gene product in the biological sample of the subject relative to a control indicates the subject has Sjögren's syndrome. Also provided is a method of treating a patient with Sjögren' s syndrome by administering to the patient a therapeutically effective amount of an agent that inhibits expression of a miR gene product that is up-regulated in the patient with Sjögren's syndrome relative to a control, or by administering to the patient a therapeutically effective amount of an isolated miR gene product that is down-regulated in the patient with Sjögren's syndrome relative to a control A method of restoring salivary flow in a patient with Sjögren' s syndrome is also provided.
EP2493889A1 IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
US20100267659 Extract obtained from orchidaceae plants, method for producing the extract, and external agent for skin comprising the extract This invention relates to an extract obtained from a plant of the genus Odontoglossum of the family Orchidaceae, or from a plant derived from a hybrid plant of the genus Odontoglossum and the genus Cochlioda, to a method for preparing the extract, and to an external agent for skin comprising the extract.
CA2625304A1 Androgen receptor related methods for treating bladder cancer Disclosed are compositions and methods for treating bladder cancer.
CN1824067A Medicine and food dual purpose product for preventing myopia and its manufacturing method A medical product used as both medicine and food for preventing and treating the myopia caused by is prepared from composite medicine, vitamins and trace elements. Its preparing process is also disclosed.
WO2013085902A1 Combination therapy methods for treating an inflammatory breast cancer Provided are combination therapy methods of treating cancer (such as an inflammatory breast cancer) comprising administering to an individual an effective amount of paclitaxel and an effective amount of romidepsin. Also provided are pharmaceutical compositions and kits comprising same.
US7153850 Lactam compounds and pharmaceutical use thereof An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, impaired glucose tolerance or adiposis, which contains a lactam compound or a pharmaceutically acceptable salt thereof as the active ingredient.
CN103405450A Application of Chukrasone A in medicaments for treating cervical carcinoma The invention discloses an application of Chukrasone A in preparing medicaments for treating cervical carcinoma, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT(3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluation finds that the Chukrasone A also has a significant inhibitory effect on the growth of human cervical carcinoma cell strains HeLa, HeLa229, HCE1 and CaSKi. Therefore, the Chukrasone A can be used for preparing anti-cervical carcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating human cervical carcinoma provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to human cervical carcinoma cells.
CN101756925B Glipizide long-acting slow-release preparation and preparation method thereof The invention provides a glipizide long-acting slow-release preparation and a preparation method thereof. A slow-release tablet taking cellulose ethers or high molecular substances as a framework material is adopted, the cost of a slow-release tablet prepared by an osmotic pump technique is greatly lowered, the preparation process is simplified, a slow-release substrate achieves linear controllable release by the improvement of the raw materials and the control of the process, the stability of a medicine is good, the time lag of 2 hours is basically achieved by a filming process, and the medicine can be better absorbed in the gastrointestinal tract. The method is simple and convenient, has low cost and is suitable for industrialized production.
CN103705445A In-situ gelling injection containing mequindox/hydrogenated castor oil The invention relates to an in-situ gelling injection containing mequindox/hydrogenated castor oil drug-loading particles, which is prepared by forming drug-loading particles from mequindox and hydrogenated castor oil and suspending the drug-loading particles in an 18-22% poloxamer 407 aqueous solution. The preparation process of the injection is simple, the drug release is uniform, the biocompatibility is good, irreversible damage to the tissue of the injection part is avoided, and the adopted sustained-release carrier can be degraded and excreted.
CN1977951B Gastrodia elata plant extract for preventing senile dementia and its preparing method The present invention relates to a gastrodia root extract containing pericin derivative and its application in preparation of medicine for preventing and curing the diseases of senile dementia. Said invention also relates to a preparation method for extracting gastrodia root to obtain its extract in which its effective component is pericin derivative. Said extract can be made into injection, tablet, capsule, seft capsule, oral liquor or dripping pills.
CN101428042A Guereza recovery plaster A medicine is mainly prepared by java brucea fruit, calomel and vinegar. A fabricating method for the medicine has the advantages of simplicity, convenient use, low cost, rapid therapeutic effect, short treatment course, no scar and no relapse. The colobus monkey healing ointment is applied to the part with flat wart or clavus when in use, and the medicine is the colobus monkey healing ointment for curing the flat wart and the clavus by clearing away heat and toxic material and removing wart.
WO2006089064A1 Methods for treating lymphomas using a combination of a chemotherapeutic agent and il-2 and optionally an anti-cd20 antibody Methods for treating B-cell lymphomas, such as non-Hodgkin's lymphoma (NHL) are disclosed. The methods use a combination therapy of a chemotherapeutic agent, an IL-2 and, optionally, an anti-CD20 antibody.
EP0854729B2 Improved methods for the production of non-covalently complexed and multivalent proteosome sub-unit vaccines A method for preparing multivalent proteosome-amphiphilic determinant vaccines suitable for parenteral or mucosal administration using diafiltration or ultrafiltration technology. The amphiphilic determinants include lipopolysaccharides from gram negative bacteria, e.g. S. flexneri, P. shigelloides and S. sonnei. Proteosomes are obtained from group B type 2b meningococci. The active proteosome-amphiphilic determinant complexes (non-covalently complexes) of the vaccine are formed using diafiltration or ultrafiltration to remove the detergent. The use of diafiltration or ultrafiltration decreases processing time and the opportunity for contamination and further permits the use of ambient temperature and efficient scale-up. In addition, the process permits the reliable and continuous monitoring of the dialysate which enhances the efficiency of the entire process. The time of dialysis for production of a lot of vaccine is reduced from > 7-10 days to less than 72 hours and usually less than 48 or 24 hours. The use of the process optimizes the presence of each antigenic component in the preparation of multivalent vaccines.
CN101786978A 2-lactamine derivative The invention relates to a 2-lactamine derivative, in particular to a novel 2-lactamine derivative and a salt thereof acceptable in pharmacy. The derivative is shown as a formula described in the specification, and R1 and R2 are defined in the specification. The invention also provides a composition containing the derivative. The 2-lactamine derivative is a dipeptidyl peptidase-IV inhibitor (DPP-inhibitor). The composition of the derivative is easy to prepare relatively, and has higher inhibitory activity for DPP-IV; therefore, the composition can be used to prevent or treat diseases related to dipeptidyl peptidase-IV (such as diabetes, obesity, hyperlipemia, and the like).
WO2008144996A1 Stable pharmaceutical cucurbitacin liquid composition Stable pharmaceutical cucurbitacin liquid compositon consisting of cucurbitacin, liquid fat and vitamin E, wherein the weight ratio of cucurbitacin and liquid is 1:100~1:5000 and vitamin E is 1%~50% of the weight of liquid fat. The said liquid fat is the fat which is liquid form in normal temperature and which is selected from the group of medium chain triglyceride(MCT), long chain triglyceride(LCT), structural oil, soybean oil, peanut oil, or olive oil, or the mixture of two or more kinds of oil therein. The liquid fat such as MCT can dissolve cucurbitacin easily and enhance the anticancer effect and decrease the individual difference. Vitamin E can enhance the stability of cucurbitacin. The stable molecular cucurbitacin liquid composition can further be prepared into soft capsule and liquid-type hard capsule which can be taken orally or externally; or the emulsion for injection, oral or external use by adding the emulsifier to the stable molecular cucurbitacin liquid composition.
CN103690555A Pharmaceutical composition for treating acetyl cholinergic urticaria The invention belongs to the technical field of treatment medicines for urticaria, and specially relates to a pharmaceutical composition for treating acetyl cholinergic urticaria and application of the pharmaceutical composition in preparation of a medicine for preventing or treating the acetyl cholinergic urticaria, aiming at overcoming the shortage that the existing medicine for treating the acetyl cholinergic urticaria has poor treatment effect and cannot act for a long time in the prior art. The pharmaceutical composition for treating or preventing the acetyl cholinergic urticaria consists of levocetirizine and isopropylidene sedoheptuiosan. The pharmaceutical composition shows a good effect on treatment of acetyl cholinergic urticaria and is remarkably worthy of clinical popularization.
CN1762357A Oral medicinal formulation of moxifloxacin and its preparation method The invention relates to an oral medicinal formulation of moxifloxacin and its preparation method, which comprises Moxifloxacin or its salt and/or its hydrate, and at least one film forming material for preparing intermediate particles of the preparation selected from hydroxy propyl methyl cellulose, hydroxy ethyl methyl cellulose, cellulose methyl, hydroxy propyl cellulose, hydroxy ethyl cellulose, sodium carboxymethyl cellulose, polyacrylic resins, polyethylene glycol, polyvinyl pyrrolidon-vinyl acetate copolymer, polyvinyl alcohol-polyethylene glycol grafted copolymer, carbopol, gelatine, poloxamer and polyvinyl pyrrolidon. The invention also discloses the process for preparing the pharmaceutical preparation.
CN103156836A Nafamostat mesilate composition and preparation method thereof The present invention relates to the field of pharmaceutical preparations, particularly to a nafamostat mesilate composition, which contains a metal ion salt, an excipient, a pH value adjustment agent and other pharmaceutically acceptable auxiliary materials, wherein the metal ion salt is one or a plurality of materials selected from potassium chloride, magnesium chloride, calcium chloride and aluminum chloride. With the composition of the present invention, quality of the nafamostat mesilate drug can be increased, drug stability can be increased, and drug efficacy can be increased.
WO2014122468A1 Combination therapy for the treatment of nosocomial pneumonia The present invention relates to a method of treatment of nosocomial pneumonia using a combination of ceftazidime (a third generation cephalosporin) and avibactam (a novel β-lactamase inhibitor), optionally with one or more additional therapeutic agents.
US20080038318 Composition; Use Of A Composition And A Method For Treating Obesity The invention relates to the use of a food-approved emulgator in the preparation of a preparation intended for the prevention of fat absorption, to a nutrient composition containing an emulgator for the prevention of fat absorption, and to a functional food characterized in that it contains an effective amount of a food-approved emulgator.
CN102317291A Fused pyrimidines Compounds of formula (I), or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6, R7, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
EP0934352B1 Water-soluble polymers for the reduction of dietary phosphate or oxalate absorption The present invention is directed to a water-soluble polyether glycol polymer having: a structural backbone of carbon atoms and oxygen atoms where there are at least two consecutive carbon atoms present between each oxygen atom; a moiety on the backbone of the polymer or a functionalized derivative on the polymer, that is cationic at physiological pH and permits complexation with phosphate or oxalate; and an average molecular weight from about 5,000 to about 750,000 Daltons. These polymers are formulated for oral dosage to reduce the phosphonate or oxalate levels in an animal. The process of preparing these polymers and the method of reducing gastrointestinal absorption of phosphate and oxalate are included.
WO2013058613A3 2-hydroxyarylamide derivative or pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition for preventing or treating cancer containing same as active ingredient The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer containing the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the invasion of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 overexpressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.
US20050222196 Azabicyclic-substituted fused heteroaryl compounds for the treatment of disease The invention provides compounds of Formula I: wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which α7 is known to be involved.
US20110293524 Methods and compositions for the regulation of lectin complement pathway (lcp)-associated complement activation in hyperglycemic myocardial damage The present invention relates to methods and compositions for regulating lectin complement pathway (LCP)-associated complement activation. In particular, the invention relates to methods and compositions for inhibiting LCP-associated complement activation in order to inhibit hyperglycemic myocardial damage. The invention also relates to the treatment of cardiomyopathy and/or hypertrophy, such as cardiac hypertrophy. The invention also relates to methods and compositions for inhibiting the loss of cardiac progenitor cells by inhibiting LCP-associated complement activation. The methods include both in vitro and in vivo methods. The methods can be accomplished by contacting a mammalian cell having a surface exposed mannose binding lectin (MBL) ligand, such as a cardiac cell, with an effective amount of a MBL inhibitor to inhibit LCP-associated complement activation.
CN101642431B Ozagrel sodium liposome injection The invention discloses an ozagrel sodium liposome injection which comprises ozagrel, sodium hydroxide, phospholipid, cholesterol, sodium deoxycholate and any pharmaceutically acceptable carrier. The invention also discloses a preferable ozagrel sodium liposome preparation which comprises the following components in parts by weight: 1 part of ozagrel, 0.175 part of sodium hydroxide, 3-20 parts ofphospholipid, 0.5-15 parts of cholesterol and 0.2-13 parts of sodium deoxycholate. The invention also discloses a method for preparing the ozagrel sodium liposome preparation, preferably an ammonium sulfate pH gradient method. The ozagrel sodium liposome preparation with high stability has high entrapment rate, low leaking rate in the process of long-term storage and devitrification-free ozagrel sodium, is suitable for industrialized production and prevents a freezing and drying process generally needed by liposome.
EP2538961A2 Methods for inhibiting necrosis A method of treating a patient suffering from a disease characterized by tissue necrosis by administering to the patient a necrosis inhibitor and/or a Humanin or a derivative of Humanin is provided. The invention further includes a method for prophylactically treating a patient at risk for a pathological condition that is precipitated at least in part by tissue necrosis by administering to the patient a necrosis inhibitor and/or a Humanin or a derivative of Humanin.
US20070287675 Enhanced Delivery of Drug Compositions to Treat Life Threatening Infections Inhalable compositions are described. The inhalable compositions comprise one or more respirable aggregates, the respirable aggregates comprising one or more poorly water soluble active agents, wherein at least one of the active agents reaches a maximum lung concentration (Cmax) of at least about 0.25 μg/gram of lung tissue and remains at such concentration for a period of at least one hour after being delivered to the lung. Methods for making such compositions and methods for using such compositions are also disclosed.
US20080147045 Use of VEGF-C or VEGF-D in Reconstructive Surgery The present invention provides materials and methods for repairing tissue and using vascular endothelial growth factor C (VEGF-C) genes and/or proteins. Methods and materials related to the use of VEGF-C for the reduction of edema and improvement of skin perfusion is provided. Also provided is are materials and methods for using VEGF-C before, during, and after reconstructive surgery.
EP1575673A2 Use of a trpm8-activating substance for the treatment of tumours The invention relates to the use of a TRPM8-activating substance for producing a pharmaceutical composition for the treatment of tumour diseases in which TRPM8 is over-expressed.
CN103110934A Method for treating diabetic gangrene The invention discloses a method for treating diabetic gangrene by adopting external bandage. When the feet of the diabetes patient are pathologically changed into foot moist gangrene, the soft tissue skin of the foot moist gangrene part is eroded to form vomica for removing much purulent secretion, the skin surrounding the moist gangrene is swelled, the method comprises the specific steps of: (1), wiping out excessive tissue of the foot gangrene part; (2), clearing the secretion in the vomica; (3), spraying anisodamine and insulinum to the vomica, so that the micro-circulation is improved and the foot gangrene blood sugar is reduced so that the foot gangrene metabolism tends to be normal, or adding powder lactobacillus plantarum capable of sufficiently generating organic acid to the vomica, so that the infection of the bacteria to the wound is effectively restrained; (4), effectively dispersing the MRM (Mechanically-Recovered Meat) ultra-micro powder for scabbing the wound to the vomica; and (5), binding up the foot gangrene part. The medicine is an external medicine which is good in treatment effect, convenient to use and capable of smoothening and flattening the healed skin.
CN101502549B Notoginsen triterpenes capsule as well as preparation method thereof and method for measuring content The invention relates to capsules of panax notoginseng saponins, a preparation method and a content determination method thereof. The contents of ingredients of panax notoginseng saponins R1, ginsenoside Rg1 and ginsenoside Rb1 in the capsules of the panax notoginseng saponins are reasonable, the efficacy is good; the preparation process is simple and easy to operate, the extraction efficiency is high, the operation cost is low, the fluidity of medicinal powder is good and the capsule content is stable. The content determination method of the invention uses the high performance liquid chromatography method to determine the contents of the three main ingredients of the panax notoginseng saponins R1, the ginsenoside Rg1 and the ginsenoside Rb1 in the capsules of the panax notoginseng saponins, thereby having strong specificity and high determination precision, solving the problems of baseline drift, incomplete separation of chromatograph peaks and the like in the chromatographic conditions for determining other preparations of the panax notoginseng saponins and further improving the quality control level of the capsules.
WO2014031762A1 Benzocyclooctyne compounds and uses thereof Provided are benzocyclooctyne compounds of formula (I). These compounds undergo strain-promoted azide-alkyne cyclo additions (SPAAC) without presence of toxic metal catalysts. The provided compounds are useful for diagnosis and imaging of azide-containing molecules. Methods for detection and imaging biomolecules using compounds of the present disclosure are disclosed.
CN101204400A Prescripton and preparing method of colla corii asini line products The invention relates to a line products of donkey-hide glue, which applies the national prescriptive drug-diet food, nutrition enhancer and food additive as raw materials, such as donkey-hide glue, IMO-900, Chinese date, silky fowl, medlar, tuckahoe, hawkthorn, calcium carbonate, calcium lactate, protohemin, ferrous lactate, vitamin A, vitamin B2, vitamin B6, vitamin C, vitamin D3, vitamin E, zinc citrate, soy isoflavones, sulfonic ester amylose. Based on the biological activity, the invention is scientifically made. The invention comprises donkey-hide glue film coated tablets, donkey-hide glue Chinese date bifido-tablets, capsule or tablet containing ass-hide glue and black-bone chicken, the formula of the donkey-hide glue multi-dimensional Ca-Fe-Zn tablets or capsule(1); the formula of the donkey-hide glue multi-dimensions Ca-Fe-Zn tablets (2); the formula of the children donkey-hide glue multi-dimensional Ca-Fe-Zn tablets or granule (1); the formula of the children donkey-hide glue multi-dimensional Ca-Fe-Zn tablets or granule (2); the formula of the children donkey-hide glue Ca-Fe tablets or granule (1); the formula of the children donkey-hide glue Ca-Fe tablets or granule (2). The invention is produced into filmy tablets or capsule or granular formulation after the pulverization, extraction, processing. The line products of donkey-hide glue has the advantages of supplying with function of nourishing yin and supplementing blood, strengthening spleen and stomach, supplying vitamin, Ca, Fe and Zn, etc., and the effectiveness is significant.
CN102702245A Hydrophobic mesoporous nanomaterial and preparation method and application thereof The invention discloses a hydrophobic mesoporous nanomaterial and a preparation method and application thereof. The hydrophobic mesoporous nanomaterial is prepared through condensation reaction of an ordered mesoporous material and a coupling reagent, wherein the coupling agent is selected from any one of the following formulae: Cl-SiR3 or RO-SiR3; and a group R contains a hydrophobic organic group. The hydrophobic mesoporous nanomaterial is introduced into a low-intensity ultrasonic system, the intensity of low-intensity ultrasonic cavitation effect can be enhanced; in-vitro and in-vivo experiments show that the hydrophobic mesoporous nanomaterial and the low-intensity ultrasonic have obvious synergistic effect and good cytocompatibility and relatively low cytotoxicity; and particularly, after solubilization, through combined use of the hydrophobic mesoporous nanomaterial with the low-intensity ultrasonic, the hydrophobic mesoporous nanomaterial can significantly inhibit the tumor growth and has a wide application prospect.
CN103601828A Complex polymer and applications thereof The invention discloses a complex polymer and applications thereof. The complex polymer is prepared from a polymer represented by formula I, and a polymer represented by formula II, and mass ratio of the polymer represented by formula I to the polymer represented by formula II is 1:1-100; in formula I, R1 and R2 represent alkyl groups containing 6-12 H or carbon atoms, and m is a number selected from 30 to 55; and in formula II, x is a natural number selected from 3 to 11, and n is a number selected from 30 to 71. The complex polymer possesses characteristics of high-temperature resistance, hypersalinity resistance, and excellent water solubility; still possesses excellent solution viscosity reducing effect at high temperatures and under hypersalinity; possesses excellent emulsifying capacity and viscosity reducing effect on crude oil; and can be widely used in the field of petrochemical industry, and especially can be used as an oil displacement agent for oil field tertiary oil recovery. The complex polymer possesses a certain degree of inhibiting effect on gram positive bacteria and gram negative bacteria.
CN101255134A Aryl pyridine compounds and medicament uses thereof The invention relates to medicinal chemistry field, more particularly, 6-aryl-3-substituted pyridone derivates with the structure represented by the formula (I) and the pharmaceutical salt thereof, and the invention further relates to a method for preparing the compounds with the structure of the formula I and the pharmaceutical use thereof. The compounds of the invention have the pharmaceutical uses for inhibiting the activity of acetylcholine esterase and preventing and curing senile dementia.
CN101595874A Validamycin amphiphilic polymer network and synthesis method thereof The invention discloses a validamycin amphiphilic polymer network and a synthesis method thereof. The validamycin amphiphilic polymer network is obtained by a chemical reaction of validamycin and hydrophobic polymer containing CH2Cl active group and swelled by a sweller, and the polymer network contains hydrophilic hydroxyl groups and hydrophobic benzene rings. The method has simple steps; the synthesized validamycin amphiphilic polymer network contains mass hydrophilic hydroxyl groups and hydrophobic benzene rings and can be swelled in different phases, which allows the Jinggangmeisu to be applied more widely.
CA2295101C Adenosine a1 receptor antagonist containing composition and method for restoring diuretic and renal function Methods and compositions for restoring diuretic and renal function comprising adenosine A1 antagonists.
CN103127028A Capsule containing fumaric acid tenofovir dipivoxil The invention aims at overcoming the defects of the technical background, and provides a capsule containing fumaric acid tenofovir dipivoxil with excellent quality and good stability, and a preparation method thereof. Compared with the prior art, the capsule disclosed by the invention has the following advantages that the capsule is slow in impurity growth, good in stability, stable in preparation technology, and good in dissolution rate in comparison with the capsule employing a hollow gelatin capsule; the same variety prepared by the technology has high bioavailability; and the capsule containing fumaric acid tenofovir dipivoxil prepared by the invention has certain advantages due to these advantages.
US20110251252 Biomarkers for mdm2 inhibitors for use in treating disease Provided herein are methods for selecting and treating a subject with leukemia, wherein the subject is selected for treatment and is treated with an MDM2 inhibitor because said subject's cells contain an FLT3-ITD mutation.
CN102438992A Method of inducing cleavage of amyloid precursor protein to form a novel fragment The present invention provides a method of inducing cleavage of amyloid precursor protein to produce an approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein in a subject, the method comprising administering a heterocyclic compound or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof, wherein the approximately 17 kilodalton fragment includes the carboxyterminal amino acid sequence of amyloid precursor protein and amyloid-beta amino acid sequence. Also provided is a screening method for identifying compounds induce cleavage of amyloid precursor protein to produce the approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein.
US20100254940 Compositions and Methods for Regulating an Immune Response in a Subject The present invention relates to compositions an methods for regulating an immune response in a subject, particularly to treat a subject with a tumor, notably a solid tumor, or an infectious disease. Disclosed are methods of regulating the innate immunity in a subject, such as by regulating the activity of γδ T cells in a subject. Disclosed are combinations of particular agents, such as a cytokine and a γδ T cell activator, particular administration regimens and dosages can produce a remarkable expansion of γδ T cells in vivo and a remarkable increase in a subject's immune defense. The invention can be used for therapeutic purposes, to produce, regulate or facilitate an immune response in a subject.
CN103086859A 2,4-dihydroxy-5,6-substituted-1-halogenobenzene derivative, synthesis method and application thereof The invention discloses a 2,4-dihydroxy-5,6-substituted-1-halogenobenzene derivative, a synthesis method and an application thereof, belonging to the field of pharmaceutical chemistry. The 2,4-dihydroxy-5,6-substituted-1-halogenobenzene derivative has the following structural general formula. The compound is of an active ingredient, and when the compound is applied to preparation of medicaments for treating, preventing or relieving complicating diseases and the like caused by obesity, the activity is better.
CN101862313A Application of anthracycline compound in preparing anti-breast cancer medicines The invention provides application of a novel anthracycline compound SZ-685C with a structure shown as a formula I in preparing anti-breast cancer medicines. The invention proves that the novel anthracycline compound SZ-685C has very strong anti-breast cancer activity through in vitro experiments and in vivo experiments. The in vivo experiments prove that the IC50 (inhibition concentrations 50) of the compound SZ-685C on breast cancer cells MCF-7 and MDA-MB-435 and human immortalized mammary epithelial cells MCF-10A after the compound SZ-685C acts for 48 hours are 3.01mu m, 7.52mu m and 49.63mu m respectively, which demonstrates that the compound SZ-685C shows the good characteristic of serving as an anti-breast cancer medicine, and the compound SZ-685C has small toxic and side effects on normal cells. Meanwhile, the in vivo experiments prove that the compound SZ-685C can obviously inhibit the growth of breast cancer transplanted tumors in a naked mouse, and the maximum tumor inhibition rate reaches more than 60 percent. Further, the anti-tumor mechanics research proves that the compound SZ-685C can induce tumor cells to die by both an endogenous way and an exogenous way which are depended by Caspase to realize the stronger anti-cancer efficiency, thereby laying the foundation for developing the novel anti-breast cancer candidate medicines with high efficiency and low toxicity. The structure of the compound is shown as the formula I.
CN101328472A Epidermal growth factor culture fluid, externally used drug for curing diabetes trauma using the culture fluid and preparation of the externally used drug The invention discloses a medicine, in particular to an epidermal growth factor culture fluid, a drug for external use which treats wounds of diabetes by adopting the culture fluid, and a preparation method thereof. Polypeptide active factors and chitosan are obtained by a gland tissue of a young of mammal through the in vitro culture process. The invention optimizes and is compatible with the polypeptide active factors and the chitosan which stimulate cell growth in different action mechanisms in order to achieve the same cooperated and intensified effects for accelerating the wound cicatrization. The product is applied to the treatment of diabetes and various wounds, has the cicatrization accelerating effect superior to the conventional treatment, and achieves satisfactory healing effects on other ulcerous skin injury. The development of the product not only provides a novel effective way for the treatment of the ulcer of diabetes wounds but also provides a better, rapider and more effective way for the conventional treatment of the wounds.
WO2008061754A1 Dietary or pharmaceutical compositions containing tricyclic diterpenes and derivatives thereof for the treatment of depression The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R1 is hydrogen or C1-6-alkyl; R2 is hydroxy, C3-5-acyloxy, hydroxymethyl, 1,3-dihydroxypropyl or C1-6-alkyl; R3 and R4 independently from each other are hydrogen, hydroxy, hydroxymethyl, C1-5- acyloxy or C1 -6-alkoxy; R5 is C1-6-alkyl, hydroxymethyl, carboxy or methoxycarbonyl; R9 is hydrogen, hydroxymethyl, methoxy, oxo or C1-5-acyloxy; R10 is hydrogen, or R5 and R9 taken together are -CH2-O- or -0-CH2-; or R5 and R10 taken together are -CO-O-, -O-CO-, -CH2-O- or -0-CH2-; R6 is hydrogen, or R5 and R6 together form a bond; R7 and R8 independently from each other are C1-6-alkyl, carboxy, x-hydroxy-Cx-alkyl (with x being an integer from 1 to 6), or C1-6-alkoxycarbonyl with the proviso that at least one of R7 and R8 is C1-6-alkyl; R11 and R12 are both hydrogen or R11 and R12 together are oxo, with the further proviso for formula (I) that if R2 is hydroxy R1 is C1-6-alkyl, for use as medicaments for the treatment of a disorder connected to impaired neurotransmission, as well as to dietary and pharmaceutical compositions and their uses.
CN101401815B Cuttlebone polysaccharide extract CBP-S and uses thereof The invention relates to the medicine technical field, in particular to a polysaccharide extract CBP-S prepared from cuttlebone and application thereof. The polysaccharide extract CBP-S mainly comprises CBP-S1 and CBP-S2, wherein in the CBP-S1, the monosaccharide ratio of Rha to Fuc to Man to Glc to Gal to GlcN to GalN is 1 to 2.8 to 1 to 6.8 to 3.2 to 2.8 to 2.2, and the monosaccharides are mainly caontained in belt-1 and 4-Glc connections; and in the CBP-S2, the monosaccharide ratio of Rha to Fuc to Man to Glc to Gal to GlcN to GalN is 1 to 5.6 to 1 to 5.6 to 2.6 to 3.6 to 2.8, and the fucose in belt-1, 4-Glc and 1,3,4 connections are mainly adopted. In animal tests, the polysaccharide extract CBP-S has protective function on the acute gastric mucosa injury, so that the polysaccharide extract CBP-S can be used to prepare a drug for protecting gastric mucosa.
CN103446091A Application of Incarviatone A in laryngeal cancer treatment drug The invention discloses application of Incarviatone A in preparation of a laryngeal cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Incarviatone A also has remarkable inhabiting effect on growth of human laryngeal cancer cell strains HEP-2, TU686, M2e and M4e. Therefore, the Incarviatone A can be used for preparation of an anti-laryngeal cancer drug and has good development and application prospect. The application of the Incarviatone A in the preparation of the laryngeal cancer treatment drug is disclosed for the first time. Due to the fact that the fact that the skeleton type is a novel skeleton type, and the high laryngeal cancer cell inhibiting activity of the Incarviatone A is previously unimagined.
WO2011096210A1 Prmt1 and prmt6 for target genes of cancer therapy and diagnosis Objective methods for diagnosing a predisposition to developing cancer, particularly bladder cancer, gastric cancer, colorectal cancer, breast cancer, esophageal cancer, lung cancer, lymphoma, pancreatic cancer and testicular cancer, are described herein. In one embodiment, the diagnostic method involves determining an expression level of PRMT1 or PRMT6 gene. The present invention further provides methods of screening for therapeutic agents useful in the treatment of PRMT1 or PRMT6 associated diseases, such as a cancer, e.g., bladder cancer, diffuse-type gastric cancer, breast cancer, esophageal cancer, NSCLC, SCLC, lymphoma, pancreatic cancer, testicular cancer, cervical cancer, osteosarcoma, prostate cancer and CML. The present invention further provides methods of inhibiting the cell growth and treating or alleviating symptoms of PRMT1 or PRMT6 associated diseases. The present invention also features products, including double-stranded molecules and vectors encoding thereof as well as to compositions containing them.
EP1713486A1 Combination therapy for dementia,depression and apathy The invention provides compositions and kits for treating dementia, depression and apathy using combination therapies involving either a monoamine oxidase inhibitor or a selective serotonin reuptake inhibitor in combination with an anti-psychotic agent.
CN103665059A Nature crocin extraction separation method and preparation for crocin blood fat reduction drug The present invention particularly relates to a nature crocin extraction separation method and preparation for a crocin blood fat reduction drug. The extraction separation method comprises: carrying out cleaning and impurity removing on dried cape jasmi fruits, extracting with deionized water, filtering to removing residue, carrying out online membrane separation and concentration fusion and macroporous absorption resin chromatography purification, and finally carrying out low-temperature spray drying to prepare the crocin. According to the present invention, the key of the invention is to create the extraction agent, and the water containing a certain auxiliary solvent is adopted to extract the crocin, wherein the extraction rate can be more than 95%; the online membrane separation and concentration fusion and the macroporous absorption resin chromatography purification are integrated; the high purity crocin production method has a characteristic of low cost and is suitable for industrial expansion production; and the compounded pharmaceutical preparation has effects of significant blood fat reduction, no side effect, effective cardiovascular and cerebrovascular related disease prevention, and blood circulation promotion, and is the preferred health care drug for crowds with high blood pressure, high blood fat and high blood sugar.
CN1615874A Penciclovir solution and its preparing method and use The water solution of penciclovir contains penciclovir in 0.2-10 g in each 1000 ml, medicinal organic solvent, water and/or buffering solution. The water solution of penciclovir has less added components, simple preparation process, high and stable penciclovir concentration, strong medicine effect, less toxic side effect and wide clinical application range.
US7618946 Analgesic compounds, extracts containing same and methods of preparation Various compounds obtained from plants of the Barringtonia species which are derived from Barringtoside A and Barringtoside C as precursor compounds which especially have an arabinopyranosyl substituent at the 21 position which may optionally be further substituted with benzoyl, dibenzoyl, methyl butanoyl, methyl butyryl or tigloyl at the 3 or 4 positions. Alternatively at the 21 position there is provided tigloyl, benzoyl or dibenzoyl substituents.
US6887905 Treatment of depression or generalized anxiety disorder A pharmaceutical composition for treating a disorder that is treated by modulation of serotonergic neurotransmission comprising administering (7S,9aS)-cis-2-Benzo[d]isoxazol-3-yl-7-(3-pyrrolidin-1-ylmethyl-phenoxymethyl)-octahydro-pyrido-[1,2-a]pyrazine and sertraline is disclosed.
CN102964351A Novel pharmaceutical salt of sitagliptin The invention relates to a novel pharmaceutical salt of sitagliptin. The novel pharmaceutical salt of sitagliptin is shown in the figure in the specification, wherein x is 1, 2, or 3, n is 0, 0.5, 1, 1.5, 2, 2.5 or 3, and R is hydrochloric acid, benzene sulfonic acid, p-toluenesulfonic acid, sulfuric acid, methylsulfonic acid, acetic acid, propanoic acid, malonic acid, oxalate, gluconic acid, succinic acid, maleic acid, fumaric acid, lactic acid, tartaric acid, malic acid, citric acid, pyruvic acid, hydroxybutyric acid, adipic acid, salicylic acid, phthalic acid, mandelic acid or benzoic acid.
CN1813771A Medicinal composition for treating skin disease and its preparing method The present invention discloses a medicine composition for curing dermopathy and its preparation method. Said medicine composition contains the following components: (by weight portion) 0.3-3.0 portions of naftifine and 0.005-0.50 portion of one component selected from halcinonide, triamcinolone acetonide acetate, betamethasone (containing betamethasone propionate and betamethasone valerate) or clobetasol propionate. Said medicine composition can be made into various medicine preparations for external application.
EP2464640A1 Inhibitors of jnk The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein p, q, Y', r, R1, R2, X, X1, X2, X3, and X4 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
US20080139523 Oxime-containing macrocyclic acyl guanidines as beta-secretase inhibitors There is provided a series of oxime-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
CN101396360A Medicine lotion for treating skin or scalp superficial part mycotic infection and preparation method thereof The invention relates to a medical lotion used for remedying skin or scalp superficial fungal infection and a preparation method thereof, in particular to a medical lotion used for remedying the superficial fungal infection caused by pityrosporum orbiculare. The combination consists of the main component of sulconazole nitrate and is applied in the form of lotion. A medical preparation using the combination has good bacteriostatic activity effect towards the pityrosporum orbiculare, can reduce the drug resistance of the pityrosporum orbiculare obviously and effectively solves the problem of the high recurrence rate.
CN101244104B Method for increasing rare saponin content in panax ginseng total saponin extract The invention provides a method for increasing the rare saponin content in the extraction of total ginsenoside, which adopts the dried root of ginseng as the raw material, wherein, the method comprises the following steps: the ginseng root is degreased, extracted and concentrated with organic reagent, and then is mixed with water and organic reagent, then is put into high-pressure steam cabinet for steaming; the ginseng root after steaming is concentrated, extracted and re-concentrated to obtain the extraction of ginsenoside with high content of rare saponin in the total ginsenoside. The obtained extraction of total ginsenoside has the advantages that the content of rare saponin comprising 20R-Rg3, 20S-Rg3,Rk1 and Rg5 is increased obviously through high-pressure liquid chromatography, wherein, the content of 20R-Rg3, 20S-Rg3,Rk1 and Rg5 is increased by 50 to 100 times than the saponin extraction of common ginseng dried root.
US7625913 Inhibitors of glycogen synthase kinase-3 (gsk-3) and aurora-2, both serine/threonine protein kinases; for treating diseases such as cancer, diabetes and alzheimer's disease This invention describes novel pyrazole compounds of formula IIIc: wherein R1 is T—Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
WO2014142127A1 Phenylxanthene derivative The present invention pertains to a compound having an excellent blood sugar lowering effect, or a pharmaceutically-acceptable salt thereof. A compound represented by general formula (I), or a pharmaceutically-acceptable salt thereof. [In the formula: R1 represents a C1-C3 alkyl group; R2 represents the same or different C1-C3 alkyl group; R3 represents an optionally-substituted pyridyl group or the like; R4 and R5 are the same or different, and each represent a C1-C3 alkyl group; R6 and R7 are the same or different, and each represent a C1-C3 alkyl group; and n represents 0 to 3.]
US7622582 Derivatives of 1-phenyl-benzofuro[3,2]pyridin-2(1H)-one 4-substituted 1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; X is NR2, O, S, SO, SO2; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, which are optionally substituted; R2 is aryl substituted with —COOR4; or R2 is: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b (b-5); -a1=a2-a3=a4- is —CH═CH—CH═CH—; —N═CH—CH═CH—; —CH═N—CH═CH—; —CH═CH—N═CH—; —CH═CH—CH═N—; wherein hydrogen atoms in (c-1)-(c-5) may be replaced by certain radicals; R3 is optionally substituted phenyl or a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted; R21 is halo, hydroxy, amino, carboxyl, C1-6alkyl, C3-7cycloalkyl, arylC1-6alkyl, formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy, —C(═O)—NR13R14; C1-6alkyloxy, arylC1-6alkyloxy, polyhaloC1-6alkyloxy, amino, mono or di(C1-6alkyl)amino, formylamino, C1-6alkylcarbonylamino, C1-6alkylsulfonylamino, mercapto, C1-6alkylthio, arylthio, aryloxy, arylC1-6alkylthio, C1-6alkylsulfynyl, C1-6alkylsulfonyl, aryl, arylamino, Het1, Het2.
CN101361722A Tacrolimus sustained release tablets and preparation method thereof The invention relates to a sustained release tablet dosage, in particular to a Tacrolimus sustained release tablet used for liver and kidney transplantation patients and a preparation method thereof, belonging to the field of medicine technology. The invention is characterized in that Tacrolimus and adhesive are taken and dissolved in ethanol to prepare Tacrolimus solution; sustained release materials, thinner and flow agent are taken, mixed and dispersed uniformly and then added into the Tacrolimus solution to prepare wet particles, which are dried, ground and added and mixed with lubricant; finally, the Tacrolimus sustained release tablet is prepared after tabletting and drying. The sustained release tablet has the unique advantages of: reducing administration times, improving the administration adaptability of patients; after administration, having stable blood concentration, small toxic and side effects and improving the drug effect and safety; reducing the total dosage of drugs so as to achieve the greatest curative effect by the lowest dosage; being capable of being realized on most of tablet production lines and easily accepted by manufacturing units and manufacturers due to relatively simple preparation process; and having relatively low manufacturing cost and broad clinical application prospect.
WO2006067311A3 Cdc25 phosphatase inhibitors The invention relates to novel compounds comprising two or three benzothiazole-4,7-diones or benzooxazole-4,7-diones units which inhibit cdc25 phosphatases, in particular an cdc25-C phosphatase. Said compounds are usable, in particular for treating cancer.
CN1771967A Oryzanol liposome and its prepn The present invention is oryzanol liposome with high absorption, high bioavailability and high stability and its preparation. The oryzanol liposome or oryzanol liposome precursor is prepared with oryzanol and phosphatide, cholesterol, supporting agent and other supplementary material. It has phosphatide/medicine weight ratio of 0.1-40, and is prepared through ethanol injecting process, film dispersion process, inverse evaporation process, extruding process or mechanical process. The supporting agent may be sorbitol, mannitol, cane sugar, etc. and has ratio to phosphatide of 0.01-400. The oryzanol liposome can act selectively on the autonomic nerve system of interbran and the center of endocrine system to improve autonomic nerve system, endocrine system and psychonerve. It is suitable for treating neurosis, climacteric syndrome, etc., and may be used in the assisting treatment of vascular headache and cerebral concussion sequelae.
US20090317403 Use of CSF-1 Inhibitors Disclosed is the use of inhibitors of CSF-1 activity for preparing a medicament for the treatment of tumor diseases.
US20100086611 Method for Treating Infectious Organisms Normally Considered to be Resistant to an Antimicrobial Drug The present invention relates to compositions of submicron- to micron-size particles of antimicrobial agents. More particularly the invention relates to a composition of an antimicrobial agent that renders the agent potent against organisms normally considered to be resistant to the agent. The composition comprises an aqueous suspension of submicron- to micron-size particles containing the agent coated with at least one surfactant selected from the group consisting of: ionic surfactants, non-ionic surfactants, biologically derived surfactants, and amino acids and their derivatives. The particles have a volume-weighted mean particle size of less than 5 μm as measured by laser diffractometry.
US20100041648 Methods for treating retroviral infections The present invention provides compositions for treating an HIV infection comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein with at least one carrier, excipient or diluent.
US8039026 Methods for treating skin pigmentation This invention relates to methods and compositions for bringing about changes in skin pigmentation. More particularly, this invention relates to compounds which affect melanogenesis and can be used as depigmenting agents or as agents for darkening skin utilizing the PAR-2 pathway.
EP1000065B1 Preparation of oxymorphone, oxycodone and derivatives The invention provides processes for the conversion of normorphinone and its derivatives, which can be synthesized from morphine, to the corresponding 14-hydroxynormorphinone and its derivatives including oxycodone, oxymorphone, noroxymorphone and naltrexone. Noroxymorphone is a key intermediate for the production of important narcotic analgesics and antagonists. The invention also provides certain novel intermediates.
US20050032771 Process for the preparation of cefixime via alkyl-or aryl-sulfonates A process for the preparation Cefixime, namely 7-[2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid, via alkyl- or aryl- sulfonates, of general formula (IA).
WO2010107704A2 Ellipticine compounds for treating obesity The present invention provides a method of reducing body weight in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I : In Formula I, R1 is H, C1-6 alkyl, or C1-6 alkyl-aryl. Each of R2 and R4 of Formula I are independently H, halogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkoxy, OR2a, SR2a, C(O)R2a, C(O)OR2a, C(O)NR2aR2b, NR2aR2b, C1-6 alkyl NR2aR2b, N(R2a)C(O)R2b, N(R2a)C(O)OR2b, N(R2a)C(O)NR2aR2b, OP(O)(OR2a)2, S(O)2OR2a, S(O)2NR2aR2b, -CN, -NO2, cycloalkyl, heterocycloalkyl, aryl or heteroaryl. Each of R2a and R2b of Formula I are independently H, C1-6 alkyl, C1-10 heteroalkyl or C1-6 alkyl-aryl. R3 of Formula I is absent, C1-6 alkyl or N-oxide. The compounds include the salts, hydrates and isomers thereof. The present invention also provides methods for the treatment of obesity and disorders related to obesity and higher than recommended percentage body fat, such as type II diabetes.
WO2009098455A1 2- (9h-xanthen-9-yl) -oxazol derivatives as m3 muscarinic receptor antagonists for the treatment of asthma and chronic obstructive lung disease The present invention relates to M3 antagonists of formula (I):wherein R1, R2, R3, R4, R5, R6, R8 and A are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment of diseases where enhanced M3 receptor activation is implicated.
US7754890 Arylsulfones and uses related thereto Aryl sulfone compounds of formula I and II are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:
EP1181042B1 Neurotrophic factors in the treatment of peripheral nerve dysfunction of pelvic area The present invention is related to a method for treating patient suffering from peripheral nerve dysfunctions in the pelvic area due to neuropathy, diabetes mellitus, acute penile trauma, penile surgery, prostatic surgery, bladder surgery or any other pelvic surgery. The invention discloses the use of neurotrophic factors, such as and their conservatively substituted variants for production of medical products acting as trophic support for treating subjects suffering e.g. from above mentioned dysfunction, including but not restricted to erectile dysfunctions. The neurotrophic factors include the proteins, nucleotide sequences encoding the proteins, their receptors, binding substances and modulators.
US8349816 Antibacterial treatment of osteoarthritis The present invention relates to use of an antibacterial agent in the manufacture of a medicament for the treatment of osteoarthritis, more particularly for the treatment of a bacterial infection which is responsible for osteoarthritis. Also described are methods for the diagnosis of osteoarthritis through the detection of certain bacteria in an affected joint of a patient with osteoarthritis.
CN1663570A Pharmaceutical composition with anti-infection, fever-relieving, pain-stopping functions The invention discloses a pharmaceutical composition with anti-infection, fever-relieving, pain-stopping functions, wherein the composition comprises active component baicalin or its corresponding water-soluble derivative and potassium dehydroandrographolide succinate or its corresponding water-soluble derivative by the weight ratio of 1-16 : 1. The invention also disclose the process for preparing clinical applicable oral preparation, injection, eye drop, liniment, nasal drop, cream by utilizing the medicinal composition.
WO2013086804A1 4-pyridyl porphyrin bridged crisscross quad-nuclear platinum complex, and preparation method and anti-tumor activity thereof Disclosed are a quad-nuclear platinum complex having a crisscross structure, a preparation method thereof, and application thereof in preparing a drug for treating human cancer. The complex is prepared through self-assembly of a single tooth platinum ligand with the chlorine ion being replaced by the nitrate and the bridging ligand being 4-pyridyl porphyrin. The preparation method is simple and easy to implement, is low in cost, can be implemented in common chemical laboratories, and does not pollute the environment during production. The complex has excellent tumor cell targeting property, induces the G-rich sequence of the oncogene to form a G-quadruplex structure, suppresses telomerase activity, and has high anti-tumor activity.
EP2401264A2 Peptoid oligomers, pharmaceutical compositions and methods of using the same Novel peptoid oligomers are disclosed that have a formula represented by the following formula I. The peptoids demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present cyclic and linear peptoids are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provoked by standard antibiotics.
CN101732311A Penfluridol-containing oral preparation and application thereof The invention relates to a penfluridol oral preparation with novel specifications. Each dosage unit contains 2.5 to 3 mg of penfluridol. When the medicament of the invention is used, the prior common method of taking 20 mg of the medicament is changed from once a week into once a day. The oral preparation is used for the maintenance treatment of schizophrenics after undergoing other psychotherapy and pharmacotherapy and having obviously relieved symptoms, prevents relapse, avoids the side effects of taking the medicament once a week, and is economical, effective and fewer in side effects than other maintaining medicaments.
CN102670707A Buccal tablet with functions of moistening throat and dispelling effects of alcohol and preparation of same The invention provides a buccal tablet with functions of moistening a throat and dispelling effects of alcohol and preparation of the buccal table. The buccal tablet comprises the following components in percentage by weight: 35 to 70% of Yunnan olive powder, 14 to 30% of flos puerariae powder, 5 to 30% of xylitol, 10 to 45% of crystal sugar, and 0.01 to 0.5% of menthol crystal, wherein the above components are mixed evenly by adding an appropriate amount of purified water and are pressed into tablets with various shapes conventionally so as to obtain the buccal tablet with functions of wetting the throat and dispelling effects of alcohol. The buccal tablet has cool and slightly sweet in entrance, has good taste, and has good effects of dispelling effects of alcohol, expelling toxin, helping produce saliva and slake thirst, clearing and moistening the throat and the like, is convenient to carry and eat, and has good health care effect if being eaten for a long time. The buccal tablet has reasonable prescription, remarkable effects, simple process and good development prospect, has easily-obtained raw materials and is particularly suitable for industrial production.
EP2217611A1 Novel modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.
US20100184742 Polymorphisms in abcb1 associated with a lack of clinical response to medicaments The present invention relates to methods, compositions, kits and reagents for determining the prognosis of a clinical response in a human patient to a medicament which acts in the central nervous system (CNS) and which is a substrate of the ABCB1 protein. Further, the invention relates to a combination of medicaments for the treatment of human patients having specific polymorphisms in the ABCB1 gene.
WO2008046796A3 Use of c10-c14-alkane-1,2-diols in the preparation of a composition for the prophylaxis and/or treatment of dermatophyte infections The present invention relates to the use of unbranched C10-C14-alkane-1,2-diols in the preparation of a composition for the prophylaxis and/or treatment of dermatophyte infections, and to cosmetic and/or dermatological preparations for topical application comprising C10-C14-alkane-1,2-diols.
CN102816100A Crystal form of prostaglandin analogue, and preparation method and application thereof The invention discloses a crystal form A of a compound having the structure shown in formula (I), and a preparation method and application thereof. An X-ray powder diffraction (XRPD) chart of the crystal form A has characteristic peaks of 2theta angels including (3.2+/-0.2) degrees, (5.4+/-0.2) degrees, (11.3+/-0.2) degrees, (16.7+/-0.2) degrees, (19.3+/-0.2) degrees, (19.8+/-0.2) degrees, (20.7+/-0.2) degrees, (22.8+/-0.2) degrees, (28.3+/-0.2) degrees.
CN1823783A Preparation method of cephapian aseptic mixed powder injection agent An aseptic mixed powder injection of a cefpiramide is prepared through respectively pulverizing aseptic cefpiramide and aseptic sodium carbonate by 100 meshes in 100-class clean region, respectively loading them in antibiotic tubular bottles, adding butyl rubber plug to them and pressing aluminum-plastic covers to said bottles.
US20120108653 Oligomers Molecules are provided for inducing or facilitating exon skipping in forming spliced mRNA products from pre-mRNA molecules in cells. The molecules may be provided directly as oligonucleotides or expression products of vectors that are administered to a subject. High rates of skipping can be achieved. High rates of skipping reduce the severity of a disease like Duchene Muscular Dystrophy so that the disease is more like Becker Muscular Dystrophy. This is a severe reduction in symptom severity and mortality.
CN103524486A N-quinolyl substituted beta-lactam compound, as well as pharmaceutical composition, synthetic method and application of compound The invention discloses an N-quinolyl substituted beta-lactam compound as shown in a general formula (I), wherein R<1> and R<2> refer to mutually independent H or C1-12 straight-chain or branched-chain hydrocarbonyl, aryl, alkoxy, acyloxy or amino; R<3> refers to H or C1-25 straight-chain or branched-chain hydrocarbonyl or aryl, or R<3> together with R<1> or R<2> forms a substituted or non-substituted five-eight-membered ring containing or without containing heteroatoms, and the heteroatoms can be N, O and S; R<4> and R<5> refer to mutually independent H or C1-12 straight-chain or branched-chain hydrocarbonyl, aryl, alkoxy, acyloxy or amino, nitryl, sulfonyl and halogen, and halogen refers to F, Cl, Br and I. The invention also provides a synthetic method of the N-quinolyl substituted beta-lactam compound, a pharmaceutical composition containing the compound, as well as application of the compound in medicine preparation of beta-lactamase inhibitors.
WO2008048340A3 Cationic steroid antimicrobial compositions for treating poxvirus infections The invention provides methods for decreasing or inhibiting poxvirus infection or pathogenesis of a cell in vitro, ex vivo or in vivo, a symptom or pathology associated with poxvirus infection or pathogenesis in vitro, ex vivo or in vivo, or an adverse side effect of poxvirus infection or pathogenesis in vitro, ex vivo or in vivo. In one embodiment, a method of the invention includes treating a subject with an invention compound (e.g., cationic steroid antimicrobial or CSA).
WO2011142246A1 Method for inhibition of potential-dependent cation channel An excellent inhibitor for a potential-dependent cation channel or an excellent masking agent; and a method for inhibiting a potential-dependent cation channel or a method for masking a sense of smell, which comprises administering an adamantane derivative represented by formula (1) or a salt thereof [in the formula, R1 and R2 are same as or different from each other, and independently represent a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and X represents -OH, -R3-OH (wherein R3 represents an alkylene group having 1 to 6 carbon atoms), -NH, -R4-NH2 (wherein R4 represents an alkylene group having 1 to 6 carbon atoms), -COOH, -R5-COOH (wherein R5 represents an alkylene group having 1 to 6 carbon atoms), -CO-R6 (wherein R6 represents an alkyl group having 1 to 6 carbon atoms), -CO-R7-COO-R8 (wherein R7 represents an alkylene group having 1 to 6 carbon atoms; and R8 represents an alkyl group having 1 to 6 carbon atoms), or NHCO-R9 (wherein R9 represents an alkyl group having 1 to 6 carbon atoms)].
US20120225862 Heteroaryl benzamides, compositions and methods of use Provided are certain heteroaryl benzamides, compositions, and methods of their manufacture and use.
CN102920766A Drug composite for treating Chinese-medicine arthralgia syndromes and preparation of patch of drug composite The invention discloses a drug composite for treating Chinese-medicine arthralgia syndromes and a preparation of a patch of the drug composite. The drug composite comprises, by weight, 100 parts of scorpio, 50 parts of red flowers, 5 parts of musk, 5 parts of borneol, 200 parts of gecko, 350 parts of yellow lead and 1800 parts of sesame oil. A certain quantity of the composite is subjected to processes such as extraction, ointment production and patch production, a transdermal patch which is easy to use and absorb is produced, and the patch has the advantages of being convenient to use, rapid in curative effect, high in cure rate and enduring in effect.
CN101139335B Use of 7-hydroxy-3-[(4-hydroxy)-3-((E)-3,7-dimethyl-octyl-2,6-diolefin)phenyl]-4H-1-benzopyran-4-ketone The present invention relates to the application of the 7-hydroxy-3-[(4-hydroxy)-3-((E)-3, 7-dimethyl-octyl-2, 6-alkenyl) phenyl]-4H-1-benzopyran-4-ketone, belonging to the medical field. The expression of ER alpha 66, ER alpha 46 and ER alpha 36 of the compound will not change under the low-concentration condition; the expression of ER alpha 66, ER alpha 46 and ER alpha 36 can be inhibited at the same time under the high-concentration condition. At the same time, the compound can kill the breast cancer cell MCF7 cell which can express the ER alpha 66, ER alpha 46 and ER alpha 36. Therefore, the compound can be used as regulator of the estrogen receptor FR alpha 36 used for treating the diseases caused by the abnormal expression of the estrogen receptor FR alpha 36, such as the tumor, osteoporosis, asthma, heart disease or Alzheimer's disease and other diseases.
WO2009088006A1 Combined pharmaceutical agent Disclosed is a pharmaceutical agent useful as a prophylactic or therapeutic agent for hypertension or a disease associated with hypertension. Specifically disclosed is a pharmaceutical agent comprising an angiotensin II receptor blocker and an insulin resistance-improving agent as active ingredients.
CN1911228A Nasal cavity gel contg. levomisole, and its new use A nasal gel of levamisol for treating allergic rhinitis chronic rhinitis, chronic nasosinusitis, adenoids, nasal polyp, etc is disclosed.
CN102579404A Sustained-release capsule containing propiverine hydrochloride and preparation method of sustained-release capsule The invention discloses a sustained-release capsule containing propiverine hydrochloride and a preparation method of the sustained-release capsule. The sustained-release capsule comprises sustained-release micropills and an empty capsule, wherein, the sustained-release micropills comprise pill cores containing drugs accounting for 75 to 97 percent and sustained-release coating layers accounting for 3 to 25 percent by weight percentage. The sustained-release capsule containing propiverine hydrochloride comprises hundreds of the sustained-release micropills with uniform particle sizes, and preparation errors or preparation defects of individual micropills cannot influence the drug release behavior of the whole preparation seriously, so that the sustained-release capsule is safer than a sustained-release tablet, the irritant activity to gastrointestinal tracts is smaller, plasma concentration is smoother, the bioavailability is higher, and the sustained-release capsule can continuously release the drugs for 24 hours if being taken for one time per day so as to treat overactive bladder. The preparation method of the sustained-release capsule prepares the pill cores containing the drugs in an extrusion and spheronization method or a drug added manner, adopts a fluidized bed to coat the sustained-release coating layers, achieves simple technology, and is easy to achieve industrialized mass production.
CN102908398A Medicinal composition for relieving female sexual fatigue The invention relates to a medical preparation, in particular to a medicinal composition for relieving female sexual fatigue. The medicinal composition is characterized in that: active ingredients of the composition consist of the following raw materials in parts by weight: 0.4-4 percent of an aqueous extract of glossy privet fruit and astragalus of equal weight, 0.1-0.3 percent of oviductus ranae, 0.1-0.5 percent of taurine and 0.05-0.5 percent of ferrous sulfate. The composition disclosed by the invention can be used for relieving female sexual fatigue, and is suitable for sportsmen, brainworkers and tourists, in particular for tourists on high plateaus to drink.
US7749488 Topical drug delivery of an aerosol foam containing benzoyl peroxide, clindamycin or salt or ester, water, surfactant, buffer, xanthan gum, emollient and propellant; non-runny, easy to apply, and uses a low residue vehicle; quick-breaking foam The present invention provides various pharmaceutically active topical delivery compositions. In particular, compositions of the present invention are present in a pressurized container comprising a quick-breaking alcoholic foaming agent, such that when the composition is released, i.e., dispensed, from the pressurized container, a quick-breaking temperature sensitive foam is formed. In addition, the present invention provides various aspects related to such compositions, including methods for modulating a foam characteristic, methods for improving the shelf-life of a pharmaceutically active compound, methods for the percutaneous treatment of various diseases, infections, and illnesses, and methods for evaluating foam characteristics.
US20070249682 Novel CD40:CD154 binding interruptor compounds and use thereof to treat immunological complications The present invention relates to novel CD40:CD154 binding interrupter compounds and use of these compounds and pharmaceutical compositions comprising them, to treat conditions associated with inappropriate CD154 activation in a subject. Specifically, this invention provides compounds which are identified by screening a library of small molecules for those that are capable of specifically binding CD154 and interrupting CD40:CD154 interaction.
CN101190215A Vitamin C chewable tablets for dog or cat The invention discloses a vitamin C chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the existing tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 10 to 30 percent of vitamin C.
US7705148 substituted diaminopyrimidine compounds having HIV inhibiting properties; reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate (4-cyano, 2-pyrimidine- aniline derivative; reaction with acrylonitril Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
US20120093748 Topical personal care and pharmaceutical compositions and uses thereof Topical compositions are provided that have 0.5% or more of at least one personal care or pharmaceutical acid, and lightly- to moderately-crosslinked PVP, which is an effective thickener in the low pH systems. In preferred embodiments, the acid is a hydroxy acid and the composition used for personal care, or prescriptive or non-prescriptive medication indications for use on the skin, hair, scalp, foot, or lips. Also provided is the use of the topical compositions to deliver the acid(s) to the skin, hair, scalp, foot, or lips. Especially preferred is a use to reduce irritation and stinging compared to an equivalent compositions not having lightly- to moderately-crosslinked PVP.
CN1895323A Jinganmin oral disintegrant tablets and preparation thereof A 'Jinganmin' oral disintegrating tablet with high curative effect is proportionally prepared from master medicine, disintegrant, filler, lubricant, and flavouring.
US20080057119 low dosage of zolpidem, or zolpidem hemitartrate when formulated for delivery across the oral mucosa, can induce rapid onset of sleep without residual sedative effects upon awakening 2-4 hours late The present invention provides compositions and methods for treating middle-of-the-night insomnia without residual sedative effects upon awakening by administering low doses (about 5 mg or less) of zolpidem or a salt thereof.
WO2006044823A2 Heteroaryl-substituted alkyne compounds and method of use The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I: wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
CN101695476A Method for preparing medical nanoparticles The invention relates to a method for preparing medical nanoparticles and belongs to the technical field of nano material preparation. The method comprises the following steps: modifying poly(amidoamine) by polyethylene glycol; modifying folic acid on the polyethylene glycol; coating quantum dots by the poly(amidoamine) modified by the polyethylene glycol and the folic acid; clamping anti-cancer medicaments into poly(amidoamine) or connecting the medicaments to the surface of the poly(amidoamine); using oil-soluble quantum dots coated by the poly(amidoamine) as nano ligands of nuclear shell structures; modifying the folic acid and polyethylene glycol on the surface of the poly(amidoamine); and positioning the poly(amidoamine) onto the surfaces of tumor cells by using the special affinity between folic acid receptors on the surface of the tumor cells and the folic acid. Meanwhile, due to the special structural characteristics of PAMAM, the internal cavities of the poly(amidoamine) can hold the anti-cancer medicaments or the surface of the poly(amidoamine) can be connected with the anti-cancer medicaments, so the toxic and side effects of the medicaments on normal tissues are reduced greatly and the stability and water solubility of the quantum dots are improved.
WO2005113763A1 Inhibition of erk-phosphorylation The present invention relates to a method for post-surgical treatment of breast cancer in women suffering from such cancer, whereby a therapeutically effective amount of an extracellular regulated kinase, (ERK-p), phosphorylation inhibitor is administered to provide for an re-expression of estrogen receptor-α (ER-α) protein and/or restoration of anti-estrogen (SERMS; selective ER modulators, SAMs; selective aromatase Inhibitors and specific estrogen receptor inhibitors as Faslodex) treatment response.
WO2011064755A1 Compositions comprising amino acids for treating chronic obstructive pulmonary disease A composition comprising leucine, isoleucine, valine, threonine and lysine for treating chronic obstructive pulmonary disease.
CN101057843A External applied spraying agent with tioconazole and its preparation method The invention relates to a tioconazole -containing exterior spraying agent, comprising tioconazole and medical findings. The weight of tioconazole is 0. 1-10% of the total weight of exterior spraying agent, and the left is medical findings. The tioconazole dissolves in the findings. The invention also discloses a method for preparing said product, which includes one step of dissolving tioconazole in the solvent. The step comprises: dissolving tioconazole in absolute ethyl alcohol and diluting tioconazole and absolute ethyl alcohol with distilled water. The invention mixed tioconazole with solvent, and forms formulation suitable for spraying agent. It overcomes problems of slow volatilization, long residual time, uneven medical distribution, slow speed of medicine reaching to injured place of paste agent, it can be used to treat tinea corporis, scald and ringworm of the nails and other body fungus infection.
CN103405433A Medicinal combination containing ilaprazole and naproxen The invention provides a medicinal combination containing ilaprazole and naproxen. The combination is formed by utilizing the ilaprazole and naproxen as active ingredients to be mixed with pharmaceutically acceptable auxiliary materials. In the combination, the weight ratio of the ilaprazole to the naproxen is (1:10)-(1:30), preferably 1:16. The medicinal combination can be made into an oral liquid for treating patients suffering from rheumatoid arthritis, ostarthritis, ankylosing spondylitis and taking the risk of gastric ulcer relapse when non-steroid anti-inflammatory drugs are taken.
CN1611224A Compound preparation of notoginseng total saponin and quzaqi aglycone and its preparing method The present invention relates to a compound preparation containing 25%-75% of notoginseng total saponin effective component and 25%-75% of Quzhaqidai (3'-hydroxyresveratrol, 4'-O-beta-D-glucopyraoside) effective component. The said effective components (or functional factors) are undergone the process of ultrafining treatment, so that its grain size is 0.001-200 micrometer. Every dosage of said compound preparation contains 50-200 mg of the effective component (or functional factor). Said invented compound preparation can promote the blood circulation and internal secretion, and has the medical action of health-protecting value for liver and some complications.
WO2011042701A1 Compositions for the prevention or treatment of migraine Compositions for the prevention or treatment of migraine are described based on the use of the low doses of particular combinations of safe natural products and the administration of different compositions in the morning and evening that contain components designed to take into account the natural circadian variation of the nutrients in the body and thereby to obtain an increase in effect with lower dosage than currently believed to be efficacious.
US20090175952 Cefuroxime axetil granule and process for the preparation thereof A cefuroxime axetil granule composition comprising a non-crystalline cefuroxime axetil solid dispersion or a substantially amorphous cefuroxime axetil, sucrose fatty acid ester, methacrylic acid-ethylacrylate copolymer and a disintegrating agent has highly desirable performance characteristics in terms of masking the bitterness of cefuroxime axetil, as well as high bioavailability and stability of cefuroxime axetil, and thus, can be advantageously used for oral administration of cefuroxime axetil.
WO2009023509A2 Therapeutic combinations useful in treating cftr related diseases The present invention relates to therapeutic combinations and kits useful in treating CFTR-related diseases, such as cystic fibrosis.
WO2013153117A1 Compositions containing probiotics and a bee pollen/clay complex, preparation method thereof and uses of same in nutrition and therapeutics The invention relates to the use of a bee pollen/clay complex as a support for the administration of probiotics, and to compositions comprising one or more probiotics and said bee pollen/clay complex.
US20110091565 Method of forming non-immunogenic hydrophobic protein nanoparticles and uses therefor Methods are described for producing non-immunogenic nanoparticles from protein sources by controlling the pH in a nanoprecipitation process. The nanoparticles that are produced by the disclosed methods range in diameter size from about 100 ran to about 400 nm, with a preferred diameter size of from approximately 100 nm to approximately 300 nm, thereby rendering them non-immunogenic. The invention further discloses methods for producing nanoconjugates that are suitable for a variety of therapeutic, diagnostic and other uses.
US20120309842 Processes for the preparation of cinacalcet The present invention provides processes and intermediates for preparing cinacalcet base and pharmaceutically acceptable salts thereof.
CA2456083C Acylthiols and component thiol compositions as anti-hiv and anti-retroviral agents Certain thiol and acylthiol compounds inhibit retrovirus growth by attacking the highly conserved zinc finger regions of essential viral proteins. These compounds, compositions containing them, and methods of using them to treat retroviral infections such as HIV are described. These compounds are also useful for preparation of vaccines comprised of inactivated retroviruses such as HIV, prevention of the transmission of such retroviruses, and detection of retroviral proteins.
EP2091909A1 Water-soluble prodrugs of florfenicol and its analogs The present invention discloses certain novel prodrugs of florfenicol and/or of florfenicol analogs, including prodrugs of salts pharmaceutically acceptable salts of florfenicol and its analogs, including nitrogen-containing esters of the secondary alcohol group of florfenicol and of its analogs, and pharmaceutically acceptable salts thereof, compositions containing them, and methods of administering them to subjects. In particular embodiments the prodrugs are sufficiently water-soluble to serve the functions needed of a water-soluble prodrug of florfenicol or of a water-soluble prodrug of a florfenicol analog. A certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing florfenicol or the florfenicol analog in question.
CN103330678A Paeonol tiny sponge preparation and preparation method thereof The invention discloses a paeonol tiny sponge preparation and a preparation method thereof, and adopts an emulsion-like menstruum diffusion method. The preparation method comprises the following steps of: preparing an inner phase, and dissolving paeonol and a polymer into a pore-foaming agent; preparing an outer phase, and uniformly stirring distilled water and an emulsion; adding the inner phase into the outer phase to stir so as to form an emulsion-like; and stirring an organic solvent so as to volatilize, and filtering and separating the organic solvent. The paeonol tiny sponge preparation prepared by adopting the class emulsion menstruum diffusion method has the advantages that the yield and encapsulation efficiency of paeonol tiny sponge are improved, the paeonol tiny sponge preparation is used for covering the skin, the effects such as efficiency, safety and long efficiency are achieved, the obtained paeonol tiny sponge preparation can permeate the deep skin so as to play the pesticide effect role for a short time, the drug action time can continue at more than 12 hours, the bioavailability is effectively improved, and the paeonol tiny sponge preparation is further used in medicine and cosmetic fields.
CN103690550A Cancer-resistant use of compound separated from tea saponin The invention relates to a cancer-resistant use of a compound separated from tea saponin and especially relates to a tea saponin compound use of proliferation inhibition and apoptosis of human gastric cancer SGC-7901 cells.
WO2006079021A2 Use of sirtuin-activating compounds for treating flushing and drug induced weight gain Provided herein are compositions and their use for treating and/or preventing flushing and/or weight gain by modulating the activity or level of a sirtuin, such as SIRTl or Sir2. Exemplary embodiments include compositions containing a sirtuin -activating compound and the use thereof for counteracting drug- induced weight gain and/or drug- induced flushing.
US7084268 producing (+)-(1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(2S,4S)-2-[(3R)-pyrrolidine-3-yl-(R)-hydroxymethyl]pyrrolidine-4-yl]thio-1-carbapen-2-em-3-carboxylic acid monohydrochloride trihydrate crystals The present invention provides carbapenem hydrochloride trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection containing them. That is, it provides carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 Å, a process for producing them, and a powdery charged preparation for injection containing them.
US7351705 Carboxylic acid compounds and a pharmaceutical agent comprising the compound as the active ingredient A carboxylic acid compound represented by formula (I): (meanings of the symbols in the formula are as mentioned in the specification) and a pharmaceutical agent comprising the compound. Since the compound represented by formula (I) binds to a DP receptor and shows antagonistic activity for the DP receptor, it is useful for prevention and/or treatment of diseases such as allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.
EP2522350A1 Use of the active ingredient combination of a 1-diethylaminoethyl-3-chinoxalin-2-on derivative and an oxysterol for breaking resistance in the treatment of cancer and strengthening the immune system against cancer, bacterial and viral diseases, autoimmune diseases, increased stress and environmental influences Composition (I) comprises an active ingredient combination of 1-(2-diethylaminoethyl)-3-(p-methoxy-benzyl)-1,2-dihydroquinoxalin-2 -one (II) and 7beta -hydroxycholesterol (III) or its salt. - ACTIVITY : Immunostimulant; Cytostatic. - MECHANISM OF ACTION : None given.
CN102579495A Drug for being externally used on skin trauma and technology for producing same A drug for being externally used on skin trauma has the technical key points that the drug consists of the following components, and the parts by weight of all the components are respectively: 1 of animal bile and 0.65-0.75 of calcium oxide. The technology for producing the drug comprises the following production steps of: (1) material preparation; (2) synthesis; (3) drying; and (4) processing. The drug has four characteristics of: 1, strong sterilization performance; 2, strong moisture absorption; 3, good protectiveness; and 4, good stability. The technology for producing the drug is simple, easy to put into production and convenient to control.
CN103251628A Application of 3beta, 22alpha-dihydroxylanosta-8,25-diene-24-one in preparing antiviral medicament The invention belongs to the field of medicines, and in particular relates to an application of 3beta, 22alpha-dihydroxylanosta-8,25-diene-24-one in preparing an antiviral medicament. Through a lot of experiments, an inventor finds that 3beta, 22alpha-dihydroxylanosta-8,25-diene-24-one has a remarkable inhibition effect on simian immunodeficiency virus (SIV), herpes simplex virus (HSV), enterovirus type 71 (EV71) and the like, so that 3beta, 22alpha-dihydroxylanosta-8,25-diene-24-one can be used for preparing a broad-spectrum antiviral medicament; and the broad-spectrum antiviral medicament contains an effective amount of 3beta, 22alpha-dihydroxylanosta-8,25-diene-24-one and a pharmaceutically acceptable carrier.
US20120077777 Ngcycloartanone derivatives with anticancer activity The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.
CN101190225A Phenobarbitone chewable tablets for dog or cat The invention discloses a phenobarbital chewable tablet used for dogs and cats. The invention overcomes the poor palatability defect of the existing tablet to promote the thorough chewing absorption by dogs and cats, so as to effectively guarantee the medicine-supply dose, to enhance the cure rate of diseases of dogs and cats and to reduce the medicine waste. The tablet of the invention comprises the following components represented by weight-percentage: 1 to 5 percent of aspartame; 20 to 30 percent of a mixture of oral dextrose and degreased milk powder; the ratio of 1:1 to 1:4 between the oral dextrose and degreased milk powder in the mixture; 40 to 60 percent of excipient; 0.5 to 1 percent of glidant and 10 to 30 percent of phenobarbital.
WO2004105768A8 Composition comprising antiprogestins and pure antiestrogens for prophylaxis and treatment of hormone-dependent diseases The present invention relates to methods and uses for preventing or treating hormone-dependent diseases, in particular breast cancer, in a mammal, by a combination of an antiprogestin, in particular the antiprogestin 11b-(4-acetylphenyl)-17b-hydroxy-17a-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, and a pure antiestrogen, in particular a compound of general formula (I) as defined in the specification, for instance 11b-Fluoro-17a-methyl-7a-{5-[methyl(8,8,9,9,9-pentafluorononyl)amino]pentyl}-estra-1,3,5(10)-triene-3,17b-diol. The invention further relates to pharmaceutical compositions comprising said combination.
WO2007005879A3 Compositions and methods for the treatment or prevention of disorders relating to oxidative stress The present invention features methods for treating or preventing conditions, diseases, or disorders related to oxidative stress. In one embodiment, the method increases Nrf2 biological activity or expression. In particular, the invention provides for the treatment or prevention of diseases relating to oxidative stress including emphysema, sepsis, septic shock, ischemic injury, cerebral ischemia and neurodegenerative disorders, meningitis, encephalitis, hemorrhage, cerebral ischemia, heart ischemia, cognitive deficits and neurodegenerative disorders.
CN101513511A Bezoar effervescent tablet for clearing away infantile lung heat, and preparation method thereof The invention relates to a bezoar effervescent tablet for clearing away infantile lung heat, and a preparation method thereof. The bezoar effervescent tablet for clearing away the infantile lung heat comprises rhizoma pinellinae praeparata, tuckahoe, Baikal skullcap roots, gypsum, bulbus fritillariae cirrhosae, radix stemonae (processed with honey), arisaema cum bile, radix cynanchi, borneol, calculus bovis factitiouscalculus bovis factitious, as well as acid agent, alkaline agent, sweetening agent, aromatic agent, lubricant and other components needed for preparing the effervescent tablet. The preparation process comprises the steps of obtaining bezoar extract powder for clearing away the infantile lung heat through water decoction, spray drying and other processes, mixing the extract powder with 10 to 20 portions of acid agent, 25 to 40 portions of alkaline agent, 2 to 5 portions of lubricant, 0 to 8 portions of sweetening agent and 0 to 4 portions of aromatic agent, tabletting and obtaining the bezoar effervescent tablet for clearing away the infantile lung heat.
CA2747992A1 Dosage regimen of an s1p receptor agonist S1 P receptor modulators or agonists are administered following a dosage regimen whereby during the initial days of treatment the daily dosage is lower than the standard daily dosage.
US7371379 Epidermal growth factors (ErbB2); gene expression inhibition; anticancer agents The present invention concerns the treatment of disorders characterized by the overexpression of ErbB2. More specifically, the invention concerns the treatment of human patients susceptible to or diagnosed with cancer overexpressing ErbB2 with anti-ErbB2 antibody.
EP2604270A1 Dextrin for suppressing elevation of blood alcohol concentration An object of the present invention is to provide an agent for suppressing elevation of blood alcohol concentration and a method for suppressing elevation of blood alcohol concentration, the agent and the method enabling prevention of an intoxication state upon drinking and further prevention of hepatic dysfunctions due to drinking such as fatty liver. Provided are an agent for suppressing elevation of blood alcohol concentration, comprising a dextrin as an active ingredient, and a method for suppressing elevation of blood alcohol concentration, comprising, when alcohol is ingested, ingesting 0.5 parts by mass or more of a digestible dextrin and/or an indigestible dextrin relative to 1 part by mass of the ingested alcohol.
WO2013056245A3 Stearate compounds Preparation and methods of treating and preventing visceral adiposity and cancer are provided involving the administration of stearate to a subject. It has been unexpectedly discovered that the fatty acid stearate, when introduced in the diet, reduces the amount of visceral fat in the body without decreasing overall body weight or causing measurable negative side effects. It has also been unexpectedly discovered that dietary stearate prevents cancer in healthy subjects and reduces both tumor size and metastasis in subjects already afflicted with cancer.
US20120015999 Formulations of (r)-1-(2,2-difluorobenzo[d] [1,3] dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl)cyclopropanecarboxamide The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith.
WO2006041019A1 Process for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride or hydrate thereof and intermediate for the same [PROBLEMS] To provide a process for industrially producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride (compound (I)), which is a compound having excellent immunosuppressive activity. [MEANS FOR SOLVING PROBLEMS] The process, which is for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride, is characterized by reacting 4-(3-benzyloxyphenylthio)-2-chlorobenzaldehyde with ethyl diethylphosphonoacetate in a solvent in the presence of a base to obtain ethyl 3-[4-(3-benzyloxyphenylthio)2-chlorophenyl]acrylate, reducing the ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, subjecting the reduced compound to mesylation, iodination, and nitration to yield 1-benzyloxy-3-[3-chloro-4-(3-nitropropyl)phenylthio]benzene, converting it to 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol with formaldehyde, and then reducing it.
CN101966150A Houttuynin derivative lipid microsphere preparation and preparation method thereof The invention belongs to the field of medicinal preparations and particularly relates to a preparation method of a lipid microsphere preparation of houttuynin and a houttuynin derivative. The lipid microsphere preparation contains the houttuynin or the houttuynin derivative. The preparation takes phospholipid and other surfactants as emulsifiers and takes high-purity plant oil as a solvent. Lipid microspheres are prepared by high-pressure homogenizing equipment. Compared with the conventional houttuynin injection, the lipid microsphere preparation avoids the application of latent solvents such as Tween and the like and remarkably improves the stability of a preparation.
CN101756902A Clonidine multivesicular liposome and preparation method thereof The invention discloses a clonidine multivesicular liposome and a preparation method thereof. The clonidine multivesicular liposome comprises clonidine serving as a medicinal active ingredient and an empty multivesicular liposome serving as a carrier. The empty multivesicular liposome comprises the following components in part by mass: 1 part of lipid component and 0.1 to 50 parts of ion gradient regulator, wherein the lipid component comprises amphiphilic lipids and neutral lipids in a molar ratio of 5-36:1. The clonidine multivesicular liposome is obtained by adopting the empty multivesicular liposome enveloped with the gradient regulator and using a transmembrane gradient active loading method to enable the clonidine to enter the aqueous phase of the empty multivesicular liposome through a phospholipid membrane. The clonidine multivesicular liposome has high utilization rate of raw materials and high loading concentation, shows good slow release effect in in vivo and in vitro experiments, and has better analgesic effect.
CN101879313A Anti-tumor nano prodrug system based on dendrimer and preparation method thereof The invention relates to a multi-function nano prodrug system based on a dendrimer, which belongs to the technical field of biomedicines and nano medical science. The nano system comprises four function parts: an outermost layer RGD (arginyl-glycocoll-aspartate) cyclic peptide as an active targeting head group (1), a polyethylene glycol (PEG) hydrophilic chain segment (2) connected with the targeting head group and the dendrimer, an anti-tumour drug (3) connected with the dendrimer by an acid sensitive chemical bond and a dendrimer kernel (4). The general formula of the nano system is RGD-PEG-Dendrimer-DOX (doxorubicine), wherein the macromolecule attribute of a dendrimer vector makes a vector system passively target to tumor tissues through an EPR (Enhanced Permeability and retention) effect; the RGD cyclic peptide makes the vector system actively target to the tumor tissues through the interaction of a ligand and a receptor and promotes the endocytosis of the tumor tissues; the acid sensitive chemical bond ensures that a drug-carrying system is stable in systemic circulation and releases active drugs after arriving tumor positions and entering an acid organelle to perform the function of cytotoxicity.
CN101032336B Pearl flavone nutrient health care food and preparation process thereof The present invention discloses one kind of pearl-flavone health food with active components comprising soybean isoflavone 50-60 weight portions, water soluble pearl powder 25-30 weight portions, taurine 8-15 weight portions, and tea polyphenol 1-5 weight portions. The pearl-flavone health food with soybean isoflavone and pearl powder capable of replenishing calcium element, and soybean isoflavone, taurine and tea polyphenol with high anti-radiation effect can raise bone density and protect body against radiation hazard. The present invention as one kind of medicated food has active components easily absorbed by human body.
US20110046090 Modulation of neurogenesis with gaba agents and gaba analogs The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a GABA agent or GABA analog, in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.
CN102241636A Derivative of ligustrazine The invention relates to the field of antithrombotic medicines, and provides a ligustrazine derivative with a structure as described in formula (I) or a pharmaceutically acceptable salt thereof. The invention also provides a preparation method for the derivative or the pharmaceutically acceptable salt thereof, a pharmaceutical composition of the derivative or the salt, and application of the derivative or the salt as an active ingredient in preparing medicines for treating cerebral thrombus, cerebral infarction, angina pectoris, myocardial infarction, coronary heart disease and arrhythmia related to thrombus.
US20080119404 angiopoietin-related growth factor used as antiobesity agent, an antidiabetic agent, and/or a hypolipidemic agent; polypeptides An antiobesity agent, an antidiabetic agent, and/or a hypolipidemic agent comprising an angiopoietin-related growth factor (AGF) or a polynucleotide encoding the same as an active ingredient a polypeptide are disclosed. Further, a functional food or a health food for alleviating obesity, diabetes, and/or hyperlipemia, comprising the AGF as an active ingredient is disclosed. Furthermore, a method for treating or preventing obesity, diabetes, and/or hyperlipemia, comprising administering to a subject the AGF or a polynucleotide encoding the same is disclosed. Furthermore, use of the AGF or a polynucleotide encoding the same in the manufacture of an antiobesity agent, an antidiabetic agent, and/or a hypolipidemic agent is disclosed.
EP1545429B1 Compositions containing citric acid for the treatment of nail fungal infections The present invention comprises methods and compositions for the treatment of pathological conditions of the dermis and dermal structures of animals and humans. In particular, the present invention comprises the use of topical delivery vehicles, including hydrogels, which incorporate active agents such as organic acids, for the treatment of dermal conditions.
EP1910302A1 Carbonyl substituted pyrazoline compounds, their preparation and use as cb1 receptor modulators The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
DE102004034573A1 Composition for treating pulmonary and coronary vascular diseases and metabolic diseases comprises L-arginine/ornithine, L-lysine, L-carnitine and L-cysteine in an isotonic sodium chloride solution Composition comprising L-arginine/ornithine, L-lysine, L-carnitine and L-cysteine in an isotonic (0.9%) sodium chloride solution, is new. - ACTIVITY : Cardiant; Vasotropic; Metabolic. No biological data given. - MECHANISM OF ACTION : None given.
US20080318943 Compounds and Uses Thereof - 848 This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. These novel compounds provide a treatment or prophylaxis of anxiety disorders, schizophrenia, cognitive disorders, and/or mood disorders.
CN103087120A Preparation method and application of monosialotetrahexosylganglioside The invention relates to a preparation method and application of monosialotetrahexosylganglioside. The method comprises the following step: by taking a cationic resin (preferably Dowex50) as a medium, in an acidic mixed water solution containing chloroform, translating a ganglioside mixture derived from an animal brain tissue into a mixture enriched with GM1. The GM1 content in the obtained translation product is increased from 7-10% before translation to 72-80%, so that the consumption of the animal brain tissue can be reduced by 7-12 times (for producing the same amount of GM1), thereby obviously lowering the production cost.
CN101579327A Azithromycin enteric capsule and preparation method thereof The invention relates to a preparation method of enteric formulation containing azithromycin particles, wherein the azithromycin particles are prepared by the following components according to the parts by weight: 110-265 of azithromycin, 0-60 of lactose, 0-60 of starch and a proper amount of sodium dodecyl sulfate and talcum powder, and the enteric formulation can be tablets, capsules and particles. The enteric formulation is rapidly released in the intestine to improve the absorption speed of medicines.
US20050009893 Administering a renin-angiotensin system inhibitor, particularly an angiotensin-receptor-blocker, an ACE-inhibitor, or a vasopeptidase inhibitor, especially incombination with a hypotensive agent A method of treating an acute cerebral vascular event (stroke) by administering a substance which inhibits the renin-angiotensin system.
US20060223868 Heterocyclic amides exhibiting and inhibitory activity at the vanilloid receptor 1(vr1) Compounds of formula I, wherein R1, n, R3, R4, R7, R8 and P are as defined in the specification, salts, solvates or solvated salts thereof, processes for their preparation, new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and the use of said compounds in therapy.
US20060122387 Derivatives of chromen-2-one as inhibitors of vegf production in mammalian cells The compounds of formula (I) wherein A and R1-R5 are as defined in the description, are inhibitors of Vascular Endothelial Growth Factor and are useful as angiogenesis inhibitors and antiproliferative agents.
US20120141596 Multi-Purpose Bio-Material Composition The present invention relates to a multi-purpose bio-material. One preferred embodiment of the present invention generally comprises KH2PO4, a metal oxide (i.e., MgO), a calcium-containing compound, a sugar and water. Exemplary calcium containing compounds include but are not limited to tri-calcium phosphates. The invented compositions has shown excellent adhesive properties as well as surprising and significant osteoproliferative properties.
CA2847022A1 Composition for the management of nausea and vomiting A pharmaceutical dosage system comprising (a) an effective amount of one or more of Doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof; (b) an effective amount of one or more of (i) Pyridoxine, (ii) an analog thereof, (iii) a derivative thereof, (iv) a prodrug thereof, (v) a metabolite thereof and (vi) a salt of any of (i)-(v); and (c) an effective amount of one or more compounds of formula (I) (see formula I) wherein R is H, PO3- or (see above formula). The system exhibits an improved pharmacokinetic profile relative to the current Diclectin®/Diclegis® formulation and is useful for example for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting of pregnancy (NVP).
CN102755327A Application of asiatic acid or salt thereof and injection suspension and preparation method thereof The invention discloses application of asiatic acid or a salt thereof and an injection suspension and a preparation method of the asiatic acid and the salt thereof. The application refers to application of the asiatic acid or the salt thereof to preparation of a medicament for preventing or treating body cavity adhesion. A formula of an injection suspension of the asiatic acid or the salt thereof comprises 0.5-10 percent of asiatic acid or the salt thereof, 0.1-1 percent of a suspending aid, 0.01-0.1 percent of a wetting agent, 0.0-5 percent of a preservative and the balance of water for injection, wherein the percentage refers to the mass percentage of each component in the total amount of the injection suspension. The injection suspension of the asiatic acid or the salt thereof can be used for effectively preventing or treating adhesion of body cavities including chest cavities, abdominal cavities, pleuroperitoneal cavities or joint cavities, and has a good wound healing effect.
US20090105321 useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma; 4-[(1S)-1-({[1-(3-chlorobenzyl)-2,3-dihydro-1H-indol-7-yl]carbonyl}amino)ethyl]benzoic acid The invention is directed to indoline amide derivatives as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included.
EP1857115A2 Using neural thread proteins to treat tumors and other conditions requiring the removal or destruction of cells The present invention is directed to methods of treating conditions requiring removal or destruction of harmful or unwanted cells in a patient, such as benign and malignant tumors, using neural thread proteins and related molecules.
US20110064789 Docosahexanoic acid as inhibitor of h. pylori The present invention concerns a method for preventing, modulating or curing in a mammal, the infections with Helicobacter pylori or the symptoms associated with H. pylori infection(s) or related diseases, and/or improving the clinical condition of a mammal infected with H. pylori, or affected by a related disease, comprising administering to a mammal in need thereof an effective amount of one or more DHA related compounds, as well as their use as an adjuvant or co-adjuvant in a method for preventing, modulating or curing in a mammal, the chronical infection with Helicobacter pylori or the symptoms associated with H. pylori infection or related diseases, and/or preventing recurrence as well as relapse of H. pylori infection or related diseases, and/or improving the clinical condition of a mammal infected with H. pylori.
CN1626078A Tindazole powder and injection preparation and preparation method A powder injection of tinidazole is prepared from tinidazole or its physiologically acceptable salt and the pharmacologically acceptable auxiliaries for injection. Its advantages are low irradiation, and high stability and quality.
CN101538302A 16alpha-methyl-3-hydroxyl-19-norpregnane-1, 3, 5-triene-20-ketone and preparation method thereof The invention relates to 16alpha-methyl-3-hydroxyl-19-norpregnane-1, 3, 5-triene-20-ketone and a preparation method thereof. In the invention, degraded product of natural diosgenine petunidin 3-acetoxyl group-pregnane-5, 16-diene-20-ketone is used as the raw material, the raw material is methylated by aluminum methide before hydrolization, 1-dehydrogenation and A aromaticcyclizationofparaflins to prepare 16alpha-methyl estrone steroid compound 16alpha-methyl-3-hydroxyl-19-norpregnane-1, 3, 5-triene-20-ketone. The compound has activity suppression effect for breast cancer cellbeads MDA-MB-231, and the preparation method is characterized by easily available raw material and high yield.
WO2008022060A3 Imidazo-pyridine derivatives for modulating protein kinase activity The present application describes compounds of formula (I) that are useful for the treatment, prevention and/or amelioration of diseases, associated with protein kinase activity. Wherein : R1 is a thiophen or a phenyl substituted with C1-C6 alkoxyl, C1-C6 alkoxyl R2 is a piperidine substituted by C(O)-R3 or R4
CN1634055A Rubitecan containing formulation for injection The invention relates to a Rubitecan containing formulation for injection which comprises Rubitecan and medical use cyclodextrin, the preparation by the invention may further includes auxiliary solvent, pH modifier and/or adjuvant for aqueous solvent for injection.
CA2643274A1 Oil-in-water emulsion composition containing licorice-derived polyphenol Disclosed is a hydrophobic licorice extract comprising mainly a middle-chain fatty acid triglyceride and a licorice-derived polyphenol contained in an amount of 1 to 50% by weight relative to the amount of the middle-chain fatty acid triglyceride. Also disclosed is an oil-in-water emulsion composition containing a licorice-derived polyphenol, which contains a polyglycerin fatty acid ester having a fatty acid residue with 14 or more carbon atoms. The composition is excellent in transparency, is stable against an acid and heat and is soluble in water, and therefore can be used in a beverage/food, pharmaceutical, quasi-drug, cosmetic or the like which can efficiently resupply a hydrophobic licorice extract such as a licorice-derived polyphenol.
WO2013114403A1 Substituted 4,5-dihydro-2h-benzo[e]indazole-9-carboxylates for the treatment of diabetes and related disorders The present invention relates to the development of novel substituted 4,5-dihydro-2H- benzo[e]indazole-9-carboxylates, which can be used as therapeutic agents for the treatment and prevention of metabolic disorders, and a process of preparing said novel compounds. More particularly, the present invention relates to substituted 4,5-dihydro- 2H-benzo[e]indazole-9-carboxylates and their related compounds, processes for preparing the said compounds and to their use in the treatment of diabetes and related metabolic disorders.
CN101496812B Compositional agent for rapid healing large-sized Acipenser sinensis with serious injury The invention relates to a quick healing group agent for large seriously injured Chinese sturgeons, relates to species conservation of the Chinese sturgeons, and needs to provide a medicine support of the quick healing group agent for quickly recovering the physique of the Chinese sturgeons. The quick healing group agent uses penicillin, streptomycin sulfate, trinosin, vitamin C, vitamin B6 and coenzyme A, and is characterized in that the dosage of each kilogram of the Chinese sturgeons comprises that: 7,547 units per kilogram of the penicillin, 4,717 units per kilogram of the streptomycin sulfate, 0.3773 milligram per kilogram of the trinosin, 4.717 milligrams per kilogram of the vitamin C, 0.2358 milligram per kilogram of the vitamin B6 and 0.4717 milligram per kilogram of the coenzyme A. The penicillin, the streptomycin sulfate, the trinosin, the vitamin B6 and the coenzyme A are dissolved into a normal saline solution or distilled water; the vitamin C is absorbed by a syringe needle tube; and the six medicines are uniformly mixed to obtain an injection solution of which the total dose is 10 milliliters.
US20110195123 Methods, compositions and systems for local delivery of drugs Implantable medical device eluting drug locally and in prolonged period is provided, including several types of such a device, the treatment modes of implementation and methods of implantation. The device comprising of polymeric substrate, such as a matrix for example, that is used as the device body, and drugs, and in some cases additional scaffolding materials, such as metals or additional polymers, and materials to enhance visibility and imaging. The selection of drug is based on the advantageous of releasing drug locally and in prolonged period, where drug is released directly to the extracellular matrix (ECM) of the diseased area such as tumor, inflammation, degeneration or for symptomatic objectives, or to injured smooth muscle cells, or for prevention. One kind of drug is the gene silencing drugs based on RNA interference (RNAi), including but not limited to si RNA, sh RNA, or antisense RNA/DNA, ribozyme and nucleoside analogs. The modes of implantation in some embodiments are existing implantation procedures that are developed and used today for other treatments, including brachytherapy and needle biopsy. In such cases the dimensions of the new implant described in this invention are similar to the original implant. Typically a few devices are implanted during the same treatment procedure.
CN101756938B Ketorolac tromethamine capsule and preparation method thereof The invention provides a ketorolac tromethamine capsule and a preparation method thereof, which belong to the technical field of medicine preparations. The ketorolac tromethamine capsule is prepared by the following steps: making ketorolac tromethamine into slow-release coated micropills and ordinary micropills; and then, uniformly and proportionally mixing the two kinds of micropills to be put into capsule cases. After the capsule enters the gastrointestinal tract, the ordinary micropills fast release medicine for taking effect, and the slow-release micropills persistently release the medicine through regulating the thickness and the materials of coated films, so the peak valley phenomenon of ordinary capsules is avoided, good release curves and repeatability can be obtained, the occurrence of untoward effects of the medicine is reduced, in addition, the medicine using times are reduced, and the adaptability of patients is improved. The preparation method of the capsule has the advantages of simple process and good controllability, and is suitable for industrial production.
US20110123459 Anaerobic Iodine Solution In accordance with the present invention, iodine, an iodine derivative(s), or a combination of a plurality of these substances is presented as the active ingredient of a stable naturopathic liquid solution. More specifically, in addition to the active ingredient, the naturopathic solution will include a liquid carrier that has been saturated with an inert gas (e.g. Nitrogen) to improve the stability of the active ingredient and increase the shelf life of the solution. For the manufacture of the solution, a liquid carrier (e.g. purified distilled water) is degassed and then subsequently saturated with the inert gas. The active ingredient is then added to the saturated liquid carrier to create the naturopathic liquid solution.
WO2010116866A1 Agent for ameliorating or preventing metabolic syndrome Disclosed is an agent for ameliorating or preventing metabolic syndrome which comprises, as the active ingredient, a degradation product of β-1,3-1,4-glucan that has a weight-average molecular weight of 1000 Da or more and less than 50000 Da. The aforesaid agent for ameliorating or preventing metabolic syndrome, which has a high biological safety and can be continuously taken everyday, is usable as a component of medical drugs, foods, drinks and so on. Also disclosed are a novel composition which is usable in preparing the aforesaid agent for ameliorating or preventing metabolic syndrome, and a method for producing the same.
WO2014003158A1 Indole derivative or salt thereof A compound represented by general formula (I) (wherein the symbols are as defined in the description) or a salt thereof has an excellent aP2 inhibitory effect and is useful as a pharmaceutical product, an aP2 inhibitor or a therapeutic agent for diseases that are ameliorated by inhibiting aP2, and the like.
US20100227919 Dioxaspiroketal Derivatives, Process for Their Preparation and Uses Thereof The invention relates to dioxaspiroketal derivatives of formula (I): wherein R, is selected from the group consisting of H, straight or branched chain C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, cycloalkyl, heterocyclyl, phenyl, optionally para-, meta- or ortho-substituted with 0 to 3 substituent selected from halogen, —CN, —NH2, —OH, —NO2, COOR2, wherein R2 is selected from H and C1-C6 alkyl, n is 1 or 2, X is O or S, R1 is selected from H, OH, halogen, C1-C6 alkyl, C1-C6 alkoxy, COOR3, wherein R3 is selected from H and C1-C6 alkyl, or physiologically acceptable salts thereof, process for preparation thereof, their uses in medical field, in particular as anti-tumour medicaments.
EP2647375A1 Combination of vargatef and dabigatran for the treatment of oncological and fibrotic diseases The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of an inhibitor of vascular endothelial growth factor receptors (VEGFRs) in conjunction with a thrombin inhibitor.
EP1634498A2 Exo-S-mecamylamine formulation A pharmaceutical composition includes a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of exo-R-mecamylamine in combination with a pharmaceutically acceptable carrier. Preferably the amount is about 0.5 mg to about 20 mg. Medical conditions are treated by administering a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of its exo-R-mecamylamine, said amount being sufficient to ameliorate the medical condition. The medical conditions include but are not limited to substance addiction (involving nicotine, cocaine, alcohol, amphetamine, opiate, other psychostimulant and a combination thereof), aiding smoking cessation, treating weight gain associated with smoking cessation, hypertension, hypertensive crisis, Tourette's Syndrome and other tremors, cancer (such as small cell lung cancer), atherogenic profile, neuropsychiatric disorders (such as bipolar disorder, depression, an anxiety disorder, schizophrenia, a seizure disorder, Parkinson's disease and attention deficit hyperactivity disorder), chronic fatigue syndrome, Crohn's disease, autonomic dysreflexia, and spasmogenic intestinal disorders.
WO2011058025A1 N-7 substituted purine and pyrazolopyrimidine compounds, compositions and methods of use The present invention relates to compounds of Formula (I) wherein R1, R2, R3, A1, A2, A3, A4, Y1 and Y2 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.
CN101401795A Imatinib mesylate orally disintegrating tablets and preparation method thereof The invention relates to the technical field of pharmaceutical preparation, in particular to an orally disintegrating tablet containing imatinib mesylate and a method for preparing the same, wherein the orally disintegrating tablet comprises effective amount of the imatinib mesylate and a pharmaceutic adjuvant which is acceptable in pharmacy and can rapidly collapse and release drugs in an oral cavity. The orally disintegrating tablet containing the imatinib mesylate has the advantages of faster action speed compared with the prior tablets and capsulated drugs, has convenient use and good taste in taking, and is more suitable for children, the elderly, and patients who can not swallow solid medicines.
US20090004166 Carrier For Enternal Administration There is provided a carrier for use in enteral administration of biologically active compounds, said carrier comprising an effective amount of one or more phosphate derivatives of one or more electron transfer agents.
CN102441167A Pharmaceutical composition having apiolin and apiolin derivant as well as histone deaceylase inhibitors and application thereof The invention relates to a pharmaceutical composition having apiolin and apiolin derivant as well as histone deaceylase inhibitors and an application in treating lung cancer, pancreatic cancer, colon cancer, liver cancer, prostatic cancer, kidney cancer, gastric cancer, brain tumor, sarcoma, ovarian cancer, breast cancer or glioma. The pharmaceutical composition provided by the invention has obvious synergistic effect, which improves the curative effect of medicine, reduces the dosage and also reduces the risk of side effect.
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